Carbon chain substances that regulate transmembrane transport and fluidity of cell membranes, their preparation and use
A water-soluble carbon chain complex addresses the challenge of finding non-toxic treatments for microbial infections by disrupting microbial cell membranes, effectively killing pathogens while sparing human cells.
Patent Information
- Application Number
- JP2025511985
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2022-05-06
- Filing Date
- 2023-05-05
- Publication Date
- 2025-05-27
AI Technical Summary
Current treatments for microbial infections lack reagents that are free of toxicity and side effects, and are unable to widely kill, prevent, or treat such infections effectively.
A water-soluble carbon chain complex is developed, comprising a lipophilic saturated and/or unsaturated carbon chain and a water-soluble portion with specific functional groups, which can bind to microbial lipid membranes or surface proteins, disrupting their structure and function to prevent or treat infections.
The complex effectively targets and kills pathogenic microorganisms without harming human cells, offering a therapeutic option for microbial infections with reduced toxicity and side effects.
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Abstract
Description
Technical Field
[0001] The present invention relates to the pharmaceutical field, and relates to water-soluble carbon chains that affect the structural function of cell membranes and the transmembrane transport of substances. Specifically, it can prevent and treat viral, bacterial, and fungal infections, and includes a carbon chain substance containing a complex capable of anti-aging and anti-inflammatory effects, a preparation method of the complex, and the use of the prepared complex in the prevention and treatment of viral, bacterial, and fungal infections, anti-aging preparations, and anti-inflammatory preparations.
Background Art
[0002] I. Structure and Function of Cell Membrane The cell membrane is one of the most important structures of organisms, mainly composed of a lipid bilayer and proteins, sugars, cholesterol, etc. embedded therein. The lipid bilayer is composed of two parallel layers of phospholipid molecules. Each layer of phospholipid molecules has a hydrophilic polar head at one end and a hydrophobic non-polar tail at the other end. Some phospholipid molecules contain various groups such as choline and glycerol, and these groups make the arrangement and spatial structure of phospholipid molecules complex and diverse. A large number of proteins are embedded in the lipid bilayer, and these proteins may pass through the entire membrane layer, cross the layer, or be partially embedded. These proteins have various functions, including messenger receptors, ion channels, enzymes, or membrane structure proteins. In addition to lipids and proteins, molecules such as sugars and cholesterol also exist on the cell membrane, and they combine with protein and phospholipid molecules through chemical reactions such as glycosylation and esterification to form complex glycoproteins and lipoproteins. Overall, the structure of the cell membrane is a semi-permeable barrier that can control and regulate the entry and exit of substances and transmit information between the inside and outside of the cell. Due to its special structure and function, the cell membrane plays an important role in life activities. The cell membrane is the outer layer of all cells and performs various functions including the following. Cell boundary: The cell membrane is the boundary between the cell and the external environment, separating the inside and outside of the cell and maintaining the stability of the cell's internal environment. Substance exchange: The cell membrane controls the entry and exit of substances, enabling the cell to obtain the substances it needs and remove waste products and toxins. This is achieved through the channels and carrier proteins in the cell membrane. Signal transduction: Receptor proteins on the cell membrane interact with external molecules and transmit information into the cell. This helps the cell to respond appropriately to external stimuli. Cell adhesion: The cell membrane adheres cells to each other to form tissues and organs. Membrane fluidity: The cell membrane is a dynamic structure, and its composition and shape are regulated by internal transport and membrane fluidity, allowing it to adapt to various environmental and physiological conditions. The cell membrane plays a very important role in maintaining the life activities of cells and adapting to the environment.
[0003] II. Fluidity of the cell membrane The fluidity of the cell membrane refers to the property of fluidity of the cell membrane, that is, the lipid molecules within the cell membrane can freely diffuse and rotate on a plane. The fluidity of the cell membrane affects the three-dimensional structure and distribution of membrane proteins on the cell membrane, and thereby can regulate cell signal transduction and the entry and exit of substances, so it is closely related to the function of the cell membrane. Furthermore, the fluidity of the cell membrane also affects the morphology and movement of cells and is involved in cell adhesion and movement. For example, cholesterol on the cell membrane affects the fluidity of the cell membrane and thereby regulates cell signal transduction and adhesion. Therefore, the fluidity of the cell membrane is an important aspect of cell membrane function. This fluidity is due to the dynamic interaction between the phospholipid bilayer structure and proteins within the cell membrane. The fluidity of the cell membrane is important for many biological processes of cells such as cell signal transduction, cell movement, and phagocytosis. Since fluidity affects the order of the lipid bilayer within the cell membrane, it affects the distribution and localization of enzymes on the membrane, and thereby can affect the activity of enzymes. Furthermore, changes in the structure and enzyme activity of the cell membrane can also affect the growth and development of living cells, cell signal transduction, and other processes. This effect usually depends on the specific function of the enzyme. For example, an enzyme may require a specific enzyme active site or may depend on a specific enzyme cofactor. Therefore, changes in the fluidity of the cell membrane can directly or indirectly affect the enzyme activity of the cell membrane, and thereby can affect the physiological and biochemical processes of cells. The cell membrane is an important isolating barrier between the inside and the external environment of the cell and is composed of a phospholipid bilayer and related proteins. When the fluidity of the cell membrane decreases, the following results can occur. Inhibition of the transport of substances within the cell: A decrease in the fluidity of the cell membrane affects the activity and mobility of transport proteins on the membrane. As a result, the transmembrane transport of substances is inhibited, and the transport rate decreases. Decrease in cell signaling: The activities of many membrane receptors and signaling molecules are related to the fluidity of the membrane. When the fluidity of the membrane decreases, the efficiency of cell signaling can decrease. Changes in the cytoskeleton: A decrease in the fluidity of the cell membrane affects the interaction between proteins on the cell membrane and the cytoskeleton, which may cause changes in the cytoskeleton. Decrease in cell adhesion and migration ability: A decrease in the fluidity of the cell membrane affects cell adhesion and may inhibit the transport of substances. Proteins and lipids within the cell membrane can move substances from the outside to the inside of the cell by means of free diffusion, etc. When the fluidity of the cell membrane decreases, these processes are inhibited, affecting the normal metabolism and functions of the cell. Improvement in the vulnerability of the cell membrane: When the fluidity of the cell membrane decreases, the phospholipid molecules of the cell membrane are arranged more closely, making the cell membrane more fragile and vulnerable to damage by substances in the external environment. Influence on cell signaling: The cell membrane is an important part of cell signaling, and signaling molecules need to bind to receptors on the cell membrane to transmit signals. When the fluidity of the cell membrane decreases, the distribution and structure of these receptors change, which may affect the normal process of cell signaling. Improvement in the permeability of the cell membrane: When the fluidity of the cell membrane decreases, the permeability of the cell membrane improves, resulting in obstacles in the process of material exchange between the internal and external environments of the cell, which may affect the normal functions of the cell. When the fluidity of the cell membrane decreases, the activity of enzymes on the cell membrane is affected. Enzymes on the membrane are usually embedded in the cell membrane, and the fluidity of the cell membrane affects the three-dimensional structure and spatial orientation of the enzyme, thereby affecting the activity of the enzyme. When the fluidity of the cell membrane decreases, the activity of these enzymes may decrease or completely stop. Therefore, the fluidity of the cell membrane is important for many biological processes within the cell. Improvement of cell membrane fluidity can have several effects on cells as follows. Improvement of cell membrane plasticity: Improvement of cell membrane fluidity means an increase in the plasticity of the cell membrane. This can make it easier for cells to adapt to environmental changes such as cell migration and morphological changes. Improvement of cell membrane permeability: When the fluidity of the cell membrane increases, the permeability of the membrane improves, making cells more sensitive to toxins, viruses, and other external factors. Enhancement of membrane protein transport: Improvement of cell membrane fluidity enhances the transport of membrane proteins. This can increase the rate of absorption and excretion of specific substances, and also increase the rate at which harmful substances enter the cell. Dysregulation of signal transduction: Improvement of cell membrane fluidity can interfere with signal transduction between cells. This can cause problems in cell growth, differentiation, apoptosis, etc. Changes in the internal and external environments of the cell membrane can change the structure and function of cell membrane proteins, so improvement of membrane fluidity can affect the enzyme activity of the cell membrane. There are many enzymes in the cell membrane, and these enzymes require the support of the lipid environment of the cell membrane to exert their enzyme activity. Changes in the fluidity of the cell membrane can affect the composition and structure of the lipid environment, thereby affecting the enzyme activity and specificity of the cell membrane.
[0004] III. Transmembrane transport through transmembrane Transmembrane transport refers to the process by which substances enter and exit cells through various mechanisms on the cell membrane. The methods of transmembrane transport include active transport, passive transport, endocytosis, and exocytosis. 1. Active transport: It is necessary to consume cell energy to transport substances from a low-concentration region to a high-concentration region. Active transport can be classified into two types: in situ active transport and secondary active transport. In situ active transport: Ions are moved from a low-concentration region to a high-concentration region through ion pumps. For example, the sodium-potassium pump transports three sodium ions from the inside to the outside of the cell and two potassium ions from the outside to the inside. Secondary active transport: The concentration difference generated by in situ active transport is utilized for the transport of other substances. For example, glucose transport proteins use intracellular ATP enzymes to transport glucose from a low-concentration region to a high-concentration region. Passive transport: Substances are transported from a high-concentration region to a low-concentration region without consuming cell energy. Passive transport can be classified into two types: simple diffusion and carrier-mediated diffusion. Simple diffusion: Small non-polar or slightly polar molecules, such as oxygen and carbon dioxide, can freely pass through the lipid bilayer of the cell membrane. Carrier-mediated diffusion: Specific substances are transported from a high-concentration region to a low-concentration region through transmembrane proteins without consuming cell energy. For example, water molecules are transported through aquaporins, and ion channels are transported through ion channel proteins. Endocytosis and exocytosis: Refer to the process by which cells take in and excrete substances through the formation of vesicles. Endocytosis and exocytosis occur through different mechanisms. Endocytosis: Cells enclose substances in vesicles and transport the substances into the cell through membrane fusion or engulfment. For example, the process by which cells phagocytize bacteria can be cited. Exocytosis: Cells enclose substances in vesicles inside the cell and excrete the substances outside the cell through membrane separation or protrusion. For example, the process by which secretory cells release insulin can be cited. Transmembrane transport refers to the process by which biomacromolecules (such as proteins and nucleic acids) on the cell membrane enter and exit cells or various organelles or regions inside the cell in a specific way. The transmembrane transport of substances refers to the process by which substances pass through the cell membrane through the mediation of membrane proteins. The factors affecting the transmembrane transport of substances are as follows. 1. Concentration gradient: The concentration gradient refers to the concentration difference of substances on both sides, and the high-concentration side diffuses towards the low-concentration side. This concentration gradient promotes the transmembrane transport of substances, especially passive transport that does not require energy consumption. 2. Molecular size and shape: The molecular size and shape affect the ability of substances to pass through membrane channels or carrier proteins. Small molecules can pass through the pores of the membrane, while large molecules need to use carrier proteins to penetrate and transport through the membrane. 3. Hydrophobicity: The membrane is composed of a lipid bilayer, and hydrophobic substances can pass through this barrier more easily. Water-soluble substances need to penetrate and transport through the membrane via carrier proteins. 4. Electrochemical gradient: The electrochemical gradient refers to the difference in the charges of substances on both sides, and charged substances are affected by the force of the electric field. This electrochemical gradient can affect transmembrane ion channels and passively transported electrokinetically. 5. The amount and activity of carrier proteins and channel proteins: Carrier proteins and channel proteins are important factors that promote transmembrane transport, and their amount and activity can affect the transmembrane transport rate of substances. In short, the transmembrane transport of substances is a complex process involving the interaction of multiple factors. If the types of substances and cells are different, the reactions to these factors may also be different.
[0005] IV. Fluidity of Cell Membrane and Transmembrane Transport The fluidity of the cell membrane is one of the important characteristics of the cell membrane structure and function. The fluidity of the cell membrane refers to the free movement of the phospholipid bilayer within the cell membrane on the cell surface, and this movement is caused by the thermal movement between phospholipid molecules. The improvement or decrease in the fluidity of the cell membrane can affect the transmembrane transport of substances. The main component of the cell membrane is the phospholipid bilayer, and within it, phospholipid molecules have fluidity. Due to the free movement of phospholipid molecules, the cell membrane can change its shape and size according to the needs of the cell and adapt to various physiological and biochemical activities of the cell. When the fluidity of the cell membrane increases, the movement of phospholipid molecules speeds up, and the fluidity of the cell membrane also increases. In this case, the three-dimensional structure of membrane proteins (such as channel proteins and carrier proteins) on the cell membrane can change, which may affect their functions. Substances need to pass through the cell membrane for transmembrane transport. The improvement of the fluidity of the cell membrane increases the movement of lipid molecules on the membrane surface, thereby increasing the diffusion rate of substances on the membrane surface, reducing the frictional force between substances and the membrane surface, and thus promoting the transmembrane transport of substances. Furthermore, many cell membrane proteins can also promote the transmembrane transport of substances by changing their three-dimensional structure, and the improvement of membrane fluidity can also affect the change of the three-dimensional structure of these proteins. Therefore, when the fluidity of the cell membrane increases, the transmembrane transport of substances is promoted in various ways. Since the functions of many transmembrane transport proteins depend on the fluidity of the cell membrane, the decrease in the fluidity of the cell membrane can affect the transmembrane transport of substances. For example, some ion channel proteins open and close channels through the fluidity of the cell membrane, and some transport proteins also require the fluidity of the cell membrane to transport substances from one side to the other. Therefore, when the fluidity of the cell membrane decreases, the functions of these proteins are affected, and the transmembrane transport of substances may be restricted.
[0006] V. Fluidity of the Cell Membrane and Cell Division and Proliferation Cell division is one of the most important events in the cell cycle and refers to the division of one cell into two or more daughter cells. There are two types of cell division: mitosis and meiosis. In mitosis, the cell's chromosomes are replicated, arranged in a structure called the spindle within the cytoplasm, and then separated into two daughter cells. In meiosis, the number of chromosomes is halved, and four cells used in the reproductive process are generated. The fluidity of the cell membrane also plays an important role in cell division. Before a cell divides, the cell membrane needs to grow and expand to enclose the two new cells during division. The fluidity of the cell membrane helps the cell in this process by enabling the expansion and shape change of the cell. Furthermore, due to the fluidity of the cell membrane, the cell can better sense the surrounding situation during division and adjust its behavior to adapt to the new environment. Therefore, the fluidity of the cell membrane plays an important role in cell division. Improvement in the fluidity of the cell membrane can play a role in cell division. Cell division is a complex biological process involving various stages of the cell cycle, changes in the cytoskeleton, chromosome separation, cytokinesis, etc. In this process, improvement in the fluidity of the cell membrane can contribute to the change in cell morphology and the progress of cytokinesis. Furthermore, improvement in the fluidity of the cell membrane may also be related to biological processes such as cell signaling and reorganization of cell membrane proteins. However, cell division and proliferation do not solely depend on the improvement of the fluidity of the cell membrane. Many other biological factors, such as the regulation of the cell cycle, DNA replication and repair, apoptosis, etc., are also involved in cell division and proliferation. Therefore, it only flows from the cell membrane. A decrease in the fluidity of the cell membrane can affect cell division and proliferation. The cell membrane is composed of a lipid bilayer and contains various lipid molecules such as phospholipids and cholesterol. The fluidity of these lipid molecules affects the structure and function of the cell membrane, thereby potentially affecting various physiological processes of the cell. Because the cell membrane plays a key role in these processes, a decrease in cell membrane fluidity can affect cell division and proliferation. For example, during cell division, the cell membrane needs to undergo significant changes to form two new cells. A decrease in cell membrane fluidity can inhibit this process and affect cell division. In addition, cell membrane fluidity is also related to cell signaling, and cell division and proliferation also depend on complex signaling pathways. However, the exact relationship between the decrease in cell membrane fluidity and cell division and proliferation is not fully understood, as this process is very complex and influenced by many different factors, and therefore much more research needs to be done to determine the specific relationship between cell membrane fluidity and cell division and proliferation.
[0007] 6. Cell membrane fluidity and cellular senescence The cell membrane is an important barrier between the inside and outside environment of the cell, and is also the main site of intracellular molecular transmission and signal transduction. The fluidity of the cell membrane refers to the free movement and exchange of molecules in the cell membrane, and is an important factor in maintaining the structure and function of the cell membrane. The changes in the cell membrane with aging include a decrease in the fluidity of the cell membrane, changes in the content and type of lipid molecules in the membrane, etc. These changes can lead to a decrease in cell function and aging. Research has shown that the changes in the content and type of lipid molecules in the cell membrane are closely related to cell aging. For example, with aging, the content of saturated fatty acids in the cell membrane increases and the content of unsaturated fatty acids decreases, which reduces the fluidity of the cell membrane and affects the function and life cycle of cells. In addition, oxidative stress can cause lipid peroxidation in the cell membrane, which destroys the integrity and fluidity of the cell membrane and affects the function and lifespan of cells. As cells age, the density and activity of receptors and channels on the membrane also change, which reduces the ability of intracellular molecular transmission and signal transduction. Therefore, maintaining the fluidity of the cell membrane can be a way to delay cell aging.
[0008] 7. Cell membrane fluidity and cell migration Improving the fluidity of the cell membrane can promote cell migration and movement. The cell membrane is composed of a lipid bilayer, and the lipid molecules within it have fluidity. The movement of these lipid molecules is regulated by the cytoskeleton and other proteins. When a cell needs to move, the structure of the cell membrane changes, thereby increasing the fluidity of the cell membrane. By enhancing the fluidity of the cell membrane, the movement and migration of cells become easier. When white blood cells need to find an infection source in the blood, they increase the fluidity of the membrane to expand the contact area and more easily pass through the blood vessel wall. Overall, increasing the fluidity of the cell membrane speeds up the diffusion rate of proteins and other molecules on the cell membrane, thereby promoting signal transduction and cell adhesion on the cell membrane and making it easier for cells to move within tissues. Furthermore, the improvement of cell membrane fluidity can also affect the cytoskeleton and the reconstruction of the cell membrane. The cytoskeleton is an intracellular scaffold structure that helps maintain the shape and stability of cells. The reconstruction of the cell membrane refers to the rearrangement of protein and lipid molecules on the cell membrane, resulting in a change in the shape of the cell. These processes are important for cell migration and movement. Since the deformation and movement of the cell membrane require the fluidity of the supporting membrane, the improvement of cell membrane fluidity promotes cell migration and movement. When a cell needs to pass through small holes or complex tissue structures, the improvement of cell membrane fluidity enables the cell to adapt to the environment and complete migration normally. When a cell expands outward, the fluidity of its membrane increases, allowing the cell to more easily pass through narrow spaces and move within the extracellular matrix. Additionally, when the fluidity of the cell membrane improves, the interaction between the cell and its surrounding environment is promoted. Receptors and channels on the cell membrane can more easily interact with extracellular molecules, thereby causing changes in signal transduction and promoting cell migration and movement. Therefore, the improvement of cell membrane fluidity is important for cell migration and movement. The movement and migration of cells require the deformation and elongation of the cell membrane, and these processes require the fluidity and flexibility of the cell membrane. A decrease in cell membrane fluidity can suppress cell movement and migration. For example, phosphatidylinositol 3,4,5-trisphosphate (PIP3) is a signal transduction molecule that plays an important role in cell polarity and movement.This study revealed that when the fluidity of the cell membrane decreases, the accumulation of PIP3 at the cell tip and cell movement and migration are suppressed.
[0009] VIII. Methods and Routes by Which Viruses Invade Cells Viral transmembrane transport refers to the process by which a virus invades a cell and transports substances such as its own genetic material or proteins from outside the cell through the cell membrane into the cell through a series of chemical and physical processes. There are many ways for a virus to invade a cell. The common methods are as follows. 1. Membrane fusion: The membrane protein on the surface of the virus binds to the corresponding protein on the cell membrane, and the virus can fuse with the cell membrane and invade the interior of the cell. 2. Endocytosis: The virus uses the receptor protein on the cell surface to recognize the cell and invade the cell. When the virus binds to the cell receptor, the cell membrane forms a vesicle that encapsulates the virus, thereby endocytosing the virus into the interior of the cell. 3. Direct penetration: Some viruses (such as poxviruses) can directly penetrate the cell membrane and invade the interior of the cell without undergoing membrane fusion or endocytosis. In any case, when a virus invades a cell, its genetic material is released, initiating an infection of the cell and enabling it to create its own copies.
[0010] IX. Methods and Routes by Which Bacteria and Fungi Invade Cells There are several ways for bacteria to invade cells. 1. Endocytosis: Some bacteria can invade cells through endocytosis. Endocytosis is a process in which cells package substances into vesicles through the cell membrane from the outside of the cell and transport them into the interior of the cell. Bacteria can utilize this process to invade cells, and most commonly, it occurs through "triggered endocytosis". 2. Pass through the cell membrane: Some bacteria, such as Rickettsia and Mycoplasma, can directly pass through the cell membrane and invade cells. 3. Active invasion: Some bacteria can invade cells through active activities using structures such as flagella, cilia, and pseudopods. 4. Toxins: Some bacteria can secrete toxins and invade cells by damaging the cell membrane, etc. These toxins can enter cells through endocytosis or other means. It should be noted that different types of bacteria have different invasion methods, and the invasion method is also affected by the interaction between bacteria and host cells. There are two main ways for fungi to invade cells. 1. Direct penetration: Fungi secrete enzymes and toxins to directly penetrate the cell membrane and cell wall of host cells and invade the interior of the cells. 2. Endocytosis: Fungi enclose host cells inside through special structures such as hyphae and pseudopods to form "food vacuoles", and then utilize endocytosis to phagocytose substances inside host cells into fungal cells. In either way, once fungi invade host cells, they use their metabolites and organelle structures for nutrient uptake, growth, and reproduction, resulting in cell damage, death, and diseases.
[0011] X. Chronic viral infections and repeated infections can cause various chronic diseases depending on the type of virus involved and an individual's immune status. Here, we introduce some common chronic diseases associated with viral infections. Hepatitis B and C viruses (HBV, HCV) are common chronic viral infections that can cause hepatitis and cirrhosis. Respiratory viral infections such as influenza virus and coronavirus can cause chronic bronchitis and emphysema. Certain viral infections such as coxsackievirus and German measles virus are thought to cause damage to pancreatic cells and insufficient insulin secretion, thereby increasing the risk of diabetes. Human immunodeficiency virus (HIV) infection can cause acquired immunodeficiency syndrome (AIDS) and other immune system-related diseases. Infection with varicella-zoster virus (VZV) can cause sequelae such as shingles and neuralgia. Parainfluenza virus infection can cause asthma and chronic obstructive pulmonary disease (COPD). Human cytomegalovirus (HCMV) infection can cause diseases in immunosuppressed patients such as post-transplant infections and reactivation.
[0012] XI. Compounds that affect cell membranes There are many compounds that affect the fluidity of the cell membrane, and the common compounds that affect the fluidity of the cell membrane are as follows. Fatty acids: The phospholipid molecules of the cell membrane are composed of two hydrophobic fatty acids and one hydrophobic phosphorylcholine or phosphorylethanolamine molecule. Fatty acids with various lengths, degrees of unsaturation, and distribution patterns affect the fluidity of the membrane, and here unsaturated fatty acids can increase the fluidity of the membrane. Cholesterol: Cholesterol is one of the most common lipids in the cell membrane and can increase the stability and rigidity of the membrane. Cholesterol decreases the fluidity of the membrane at low temperatures but increases the fluidity of the membrane at high temperatures. Phosphatidylinositol: Phosphatidylinositol is a minor component of the cell membrane that regulates cell signaling and the fluidity of the cell membrane. Phospholipids: The cell membrane is mainly composed of phospholipids, and various types of phospholipids can affect the fluidity of the cell membrane. Alcohol: Alcohol can damage the structure of the cell membrane and affect the fluidity and stability of the cell membrane. Squalene: Squalene is a substance similar to cholesterol, which can increase the fluidity of the cell membrane and improve the softness of the cell membrane. Choline: Choline is a type of vitamin B group, which can promote the fluidity of the cell membrane and has an antioxidant effect. Tartaric acid: This is a natural organic acid that can decrease the fluidity of the cell membrane and affect the function of the cell. Citric acid: This is also a natural organic acid that can decrease the fluidity of the cell membrane. Surfactants: These compounds can interact with the cell membrane and decrease the fluidity of the cell membrane. Non-ionic surfactants: These compounds have the same effect as surfactants but interact with the cell membrane more gently. Among many microorganisms, pathogenic microorganisms that can directly cause human diseases are generally viruses, bacteria, and fungi. Except for some non-enveloped viruses, most microorganisms have a lipid membrane. The lipid membrane of microorganisms has the same functions as the cell membranes of other organisms. Structurally, it is composed of a phospholipid bilayer as the basic framework of the membrane, and proteins penetrate, insert, and adhere to the surface of the phospholipid bilayer. On the outer surface of the membrane, there are glycoproteins composed of proteins and a small amount of polysaccharides, and there are also some saccharides that combine with lipids to form glycolipids. The lipid membrane of microorganisms is usually 7 to 8 nm, has a certain degree of fluidity, and not only serves as a barrier to create a stable internal environment for the life activities of microorganisms, but also has semi-permeability and selective permeability. That is, substances can selectively enter cells through diffusion, osmosis, active transport, etc., thereby ensuring the normal metabolism of cells. The present invention relates to a group of complexes and their preparations that target the destruction and influence of the structure and function of the lipid membrane of microorganisms or the nucleocapsid of non-enveloped viruses.
[0013] 1. Virus 1.1 Enveloped Viruses and Non-Enveloped Viruses Viruses are the smallest infectious particles in which one or more nucleic acid (DNA or RNA) molecules are enclosed in a protein shell, and they are non-cellular microorganisms that can only replicate themselves inside living cells with high sensitivity. Outside the cell, viruses exist in the form of particles, and a structurally complete infectious virus particle is called a virion. All viral genomes are surrounded by a protein shell, and this structure is called a nucleocapsid, and the protein shell is called a capsid. The basic structure of a virion is a nucleocapsid, but some viruses have a double-layer lipid envelope outside the nucleocapsid. Such viruses are called enveloped viruses, and viruses without an envelope are called naked viruses. 1.2 Structure and Function of the Virus Envelope The envelope is the cytoplasmic membrane obtained when a virus is released from a host cell and may also be an intracellular organelle membrane or a nuclear membrane. Therefore, the viral envelope has specific characteristics of the host cell membrane, enabling the virus to exhibit a specific "affinity" for the host cell membrane. The envelope contains a bilayer of lipids and several proteins called envelope proteins encoded and synthesized by viral genes. These are virus-specific and often form subunits of polysaccharides and glycoproteins, embedded in the lipid layer, and on the surface, there are knob-like protrusions called "Spike or Capsule particles". They are located on the surface of the virion, highly antigenic, can selectively bind to host cell receptors, promote the fusion of the viral envelope and the host cell membrane, and enable the infectious nucleocapsid to enter the cell and cause infection. Therefore, the envelope proteins of enveloped viruses determine the infectivity of the virus, while the nucleocapsid of enveloped viruses is the nucleus of the virus and has no infectivity when present alone, i.e., when the envelope is lost. 1.3 Structure and Function of Non-Enveloped Viruses Since naked viruses have no envelope, their nucleocapsid is the mature virus, and its infectivity is determined by the capsid protein. The capsid protein is a viral gene product that gives the virus its unique shape and protects the internal nucleic acid from damage by nucleases in the external environment (such as blood). At the same time, the capsid protein has a function to assist in infection. The specific receptor-side connexins on the virus surface have a special affinity for the corresponding receptors on the cell surface, which is the first step for the virus to selectively adsorb to the host cell and establish an infection source. The capsid protein also exhibits virus-specific antigenicity and can stimulate the body to cause an antigen-virus immune response. 1.4 Types of Enveloped Viruses Enveloped viruses include influenza virus, coronavirus, human immunodeficiency virus, hepatitis B virus, hepatitis C virus, rabies virus, herpes virus, Ebola virus, hantavirus, dengue virus, Japanese encephalitis virus, Zika virus, etc. The immune system relies on proteins on the cell membrane to distinguish between enemies and allies. Enveloped viruses are recognized as allies by the host immune system simply because they have an extra lipid membrane layer. The glycosylation modification of envelope proteins, on the one hand, exerts an antigen masking effect, making vaccine development more difficult. On the other hand, the modified glycan brings about a spatial reconstruction effect on the antigen epitope structure. 1.5 Coronavirus Coronavirus: A total of seven coronaviruses that can infect humans, namely HCoV-229E, HCoV-OC43, SARS-CoV, HCoV-NL63, HCoV-HKU1, MERS-CoV, and SARS-CoV-2 have been discovered. The diameter of the coronavirus is about 60 to 220 nm. The virus has an envelope structure, and there are three proteins on it, namely spike glycoprotein (S protein), small envelope glycoprotein, and membrane glycoprotein (M protein). Also, some types have hemagglutinin glycoprotein (HE protein). The S protein recognizes and binds to the host cell surface receptor and plays an important role in mediating the fusion of the virus envelope and the cell membrane. The M protein is involved in the formation and budding process of the virus envelope, and the HE protein is a short protrusion that constitutes the envelope and may be related to the initial adsorption of the coronavirus. The HE protein of some coronaviruses may cause the aggregation and adsorption of red blood cells. 1.6 Treatment of Coronavirus The vaccines and therapeutic drugs for novel coronavirus infection currently in clinical development are mainly classified into the following four categories. The first type is small-molecule antiviral drugs, including Merck's Molnupiravir, Pfizer's Paxlovid, Shionogi & Co., Ltd.'s Ensitrelvir, as well as commercially available drugs such as remdesivir, lopinavir / ritonavir, and favipiravir. Small-molecule drugs such as lopinavir / ritonavir are widely used in antiviral treatment but are not specific drugs for treating coronavirus disease 2019 (COVID-19). The second type is anti-inflammatory drugs. Many biological agents such as tocilizumab and siltuximab are used to suppress cytokine storms. In addition, clinical trials of small-molecule anti-inflammatory drugs such as baricitinib and ruxolitinib are also being conducted. The third type is neutralizing antibodies. This refers to antibodies that can eliminate the infectivity of the virus after binding to the virus. Its mechanism of action is to change the surface structure of the virus, prevent the virus from adsorbing to cells that are easily infected, prevent the virus from invading and multiplying in cells, and the immune complex formed by the virus and the neutralizing antibody is easily phagocytosed and removed by macrophages. The fourth type is vaccines, including five types such as recombinant protein vaccines, nucleic acid vaccines, viral vector vaccines, inactivated vaccines, and live attenuated vaccines. 1.7 Non-enveloped viruses Non-enveloped naked viruses include hepatitis A virus, human papillomavirus, adenovirus, poliovirus, coxsackievirus, etc. Human papillomavirus (HPV) belongs to the genus Papillomavirus of the family Papillomaviridae and is a spherical, non-enveloped double-stranded DNA virus with a diameter of 52 to 55 nm. The viral genome is a double-stranded circular DNA of approximately 7.8 to 8.0 kb and is divided into an early region, a late region, and a regulatory region. The early region encodes proteins (such as E5, E6, E7, etc.) related to viral replication, transcriptional regulation, and cell transformation, and the late region encodes the major capsid protein L1 and the minor capsid protein L2. More than 130 types have been isolated so far, causing different clinical symptoms depending on the type, and are divided into low-risk types of the skin, high-risk types of the skin, low-risk types of the mucosa, and high-risk types of the mucosa according to the infiltrated tissue site. Skin HPV infections such as common warts, plantar warts, and flat warts are very common among people, but specific infection rates cannot be obtained.
[0014] 2 Bacteria The basic structure of bacteria includes a cell wall, a cell membrane, cytoplasm, and nucleoid. 2.1 Bacterial Cell Membrane The bacterial cell membrane is an elastic semi-permeable membrane composed of a phospholipid bilayer and chimeric proteins. The membrane is 8 to 10 nm thick and the outer side is in close contact with the cell wall. The absence of cholesterol in the bacterial cell membrane distinguishes it from the cell membranes of eukaryotes. The bacterial cell membrane contains a rich enzyme system that performs many important metabolic functions. The multifunctionality of the bacterial cell membrane is a very important feature different from other cell membranes. For example, the inner side of the cell membrane contains an enzyme system for electron transport and oxidative phosphorylation and can perform part of the functions of the mitochondria of eukaryotic cells. Structural characteristics of the bacterial cell membrane: (1) The main body of the membrane is a lipid bilayer. (2) The lipid bilayer has fluidity. (3) Integral proteins "dissolve" in the hydrophobic inner layer of the lipid bilayer because their surfaces are hydrophobic. (4) Since the surfaces of peripheral proteins contain hydrophilic groups, they can be connected to the polar heads on the surface of the lipid bilayer by electrostatic attraction. (5) There are no covalent bonds between lipid molecules or between lipid and protein molecules. (6) The lipid bilayer is like a "sea" in which integral proteins sink like "icebergs" and move laterally, while peripheral proteins can "float". Physiological functions of the bacterial cell membrane: (1) It can selectively control the transport of nutrients and metabolites inside and outside the cell. (2) It is a structural barrier for maintaining the normal osmotic pressure inside the cell. (3) It is the main site for synthesizing cell wall and glycocalyx-related components (such as peptidoglycan, teichoic acid, LPS, capsular polysaccharides, etc.). (4) Enzyme systems related to energy metabolism such as oxidative phosphorylation and photosynthetic phosphorylation exist in the membrane, serving as the energy production base of the cell. (5) This is the insertion site of flagella and provides the energy required for flagellar rotation. 2.2 Bacterial cell wall The main component of the cell wall is peptidoglycan, also known as murein. Peptidoglycan is a polysaccharide scaffold formed by the β-1,4 glycosidic bond connection of two amino sugars, N-acetylglucosamine and N-acetylmuramic acid, which are arranged at intervals. The tetrapeptide side chains are bound to N-acetylmuramic acid molecules, and the peptide chains are linked by peptide cross-links or peptide chains, forming a highly mechanical network structure. 2.2.1 Gram-positive bacteria Gram-positive bacteria have a thick cell wall, about 20 to 80 mm. Peptidoglycan is rich in content, with 15 to 50 layers, each layer being 1 nm thick, accounting for about 50 to 80% of the dry weight of the cell wall. Furthermore, it contains a large number of teichoic acids, which are special components. Teichoic acids have strong antigenicity and are important surface antigens of Gram-positive bacteria. They play a role in controlling the passage of ions through the mucopeptide layer. They may also be related to the activity of specific enzymes. The teichoic acids of certain bacteria may adhere to the surface of human cells and act like cilia, which may be related to pathogenicity. 2.2.2 Gram-negative bacteria The cell wall of Gram-negative bacteria has a multi-layered structure. The cell wall is thin, about 10 to 15 nm, with 1 to 2 layers of peptidoglycan, accounting for about 5 to 20% of the dry weight of the cell wall. Outside the cell wall, there is also an outer membrane of bacteria composed of proteins, phospholipids, and lipopolysaccharides. The outer membrane has a lower phospholipid content but a higher lipopolysaccharide content than the cytoplasmic membrane. The proteins in the outer membrane, unlike those in the cell membrane, have one end covalently bonded to the tetrapeptide side chain of peptidoglycan by a protein moiety, and the other end covalently bonded to the phosphate of the outer membrane through a lipid moiety. Its function is to stabilize the outer membrane and fix it to the peptidoglycan layer. Lipopolysaccharide is known as the endotoxin of bacteria and exists in the outermost layer of the outer membrane. The outer membrane is the main structure of the cell wall of Gram-negative bacteria. In addition to transporting nutrients, it also has a barrier function to prevent the penetration of many substances and resist the influence of many chemicals. 2.3 Antibiotics Antibiotics are mainly secondary metabolites produced by bacteria, fungi, or other microorganisms, or artificially synthesized analogs. They are mainly used for the treatment of various bacterial infections or pathogenic microorganism infections and generally do not cause significant side effects to the host. The mechanism of action of antibiotics generally includes inhibiting the synthesis of bacterial cell walls, causing bacteria to expand, rupture, and die in a low osmotic pressure environment; interacting with the bacterial cell membrane, increasing the permeability of the bacterial cell membrane, opening ion channels on the membrane, causing useful substances inside the bacteria to leak out of the bacteria, or disrupting the electrolyte balance to kill bacteria; interacting with bacterial ribosomes or their reaction substrates (such as tRNA, mRNA) to inhibit protein synthesis, so that structural proteins and enzymes necessary for cell survival cannot be synthesized; and inhibiting the replication and transcription of bacterial DNA, interfering with the processes of bacterial cell division and regeneration, transcription and translation into proteins. 2.4 Antibiotic Resistance It is well known that the excessive, high-dose, and long-term use of antibiotics can lead to the emergence of drug resistance. In order to deal with pathogenic microorganisms, new antibiotics are continuously being developed. However, microorganisms such as bacteria gradually adapt to this drug environment in order to survive, continue to mutate to form stronger new bacteria, and the cycle continues. There are even multi-drug resistant bacteria, that is, bacteria in which one type of bacteria is simultaneously resistant to three or more antibiotics. Further research has shown that bacteria show resistance because they have resistance genes in their bodies. NDM-1 is a newly discovered super resistance gene by scientists, encoding a new drug-resistant enzyme NDM-1 with the full name "New Delhi metallo-β-lactamase 1". This enzyme is a very efficient enzyme that can decompose and inactivate most antibiotics. Resistance genes not only confer resistance to the bacteria themselves but can also spread in the environment and transfer to other bacteria to confer resistance to antibiotics. Currently, there are few available new antibiotics, and existing antibiotics cannot effectively kill drug-resistant bacteria. Therefore, when infected with drug-resistant bacteria, the risk of patient death is significantly increased, and the mortality rate of patients infected with drug-resistant bacteria is about twice that of patients infected with non-resistant bacteria. Therefore, the infection and spread of drug-resistant bacteria have become a major issue in modern medicine.
[0015] 3. Fungi, Chlamydia, and Mycoplasma The basic structure of fungal cells includes a cell wall, cell membrane, nucleus, endoplasmic reticulum, mitochondria, etc. The main component of the fungal cell wall is chitin. The fungal cell membrane is also composed of a phospholipid bilayer, but the plasma membrane contains sterols, and ergosterol plays an important role in maintaining membrane permeability and fluidity. Antifungal drugs include three types: polyenes (amphotericin B preparations), triazoles (voriconazole, itraconazole, posaconazole), and echinocandins (caspofungin, micafungin, anidulafungin). Chlamydia is a Gram-negative pathogen that has a cell wall and cell membrane but no peptidoglycan, and polypeptides linked by disulfide bonds serve as scaffolds. Mycoplasma has no cell wall and only a cell membrane composed of a phospholipid bilayer, which plays a certain role in maintaining the integrity of the cell membrane.
[0016] 4. Targeting the lipid membrane components of microorganisms The main structure of the lipid membrane of microorganisms is a phospholipid bilayer, and its main components are phospholipids, proteins, and polysaccharides. By disrupting the continuity and stability of the lipid membrane of microorganisms, the membrane permeability can be changed, increased, and an antimicrobial role can be played. 4.1 Structure and composition of the cell membrane of microorganisms The thickness of the lipid membrane of microorganisms is generally 7 to 8 nm. The lipid membrane is mainly composed of lipids and proteins. Lipids account for 50%, proteins account for 40%, and polysaccharides account for about 1 to 10%. Membrane lipids mainly include phospholipids and glycolipids, where phospholipids account for more than about 50% of the membrane lipids. Phospholipids are mainly glycerophospholipids. With glycerol as the backbone, two fatty acid chains and one phosphate group are bound to this backbone, and molecules such as choline, ethanolamine, serine, or inositol are bound to the lipid molecule via the phosphate group. The hydrophilic end of the phospholipid molecule is the phosphate group called the head, and the hydrophobic end of the phospholipid molecule is two hydrocarbon chains of different lengths called the tail, usually containing 14 to 24 even-numbered carbon atoms. Here, one or more double bonds are often contained in one of the hydrocarbon chains, and the presence of the double bond causes this unsaturated chain to twist at a specific angle. The content of glycolipids is about 5% or less of the membrane lipids. The simplest glycolipid is galactosylceramide, which has only one galactose as the polar head, and glycolipids play a role in integrating membrane proteins. 4.2 Microbial membrane lipids This is the basic framework of the membrane. When the membrane lipids are removed, the membrane collapses. Membrane lipids are the solvent for membrane proteins. Some proteins interact with membrane lipids through their hydrophobic ends, and the proteins are embedded in the membrane to perform special functions. Membrane lipids provide an environment for specific membrane proteases to maintain their three-dimensional structure and express their activity. The activity of many enzymes on the membrane depends on the presence of membrane lipids. 4.3 Membrane proteins of microorganisms Membrane proteins account for 40% to 50% of the membrane. The more complex the membrane function is, the higher the protein content on the membrane. Depending on how membrane proteins bind to membrane lipids and their positions within the membrane, membrane proteins are classified into integral proteins, peripheral proteins, and lipid-anchored proteins. Some or all of the integral proteins are proteins embedded within or on both sides of the cell membrane. Since they are very strongly bound to the membrane, they can only be washed out of the membrane with detergents, such as the commonly used SDS and Triton-X100. Peripheral proteins, also called extrinsic proteins, are water-soluble and are distributed on the surface of the cell membrane. They are bound to the hydrophilic parts of protein molecules or lipid molecules on the membrane surface by ionic bonds or other weak bonds, so they can also be separated from the membrane by changing the ionic strength of the solution or raising the temperature. Lipid-anchored proteins, also known as lipid-linked proteins, bind to lipids in two ways. One is to bind indirectly to lipids within the lipid bilayer via sugar molecules, and the other is for the protein to bind directly to lipids within the lipid bilayer. Lipid-anchored proteins are fixed via phospholipids or fatty acids and are covalently bonded. Membrane proteins have functions such as transport, catalyzing related metabolic reactions, binding proteins, and receptors. 4.4 Microbial Membrane Carbohydrates Microbial membrane carbohydrates account for 2% to 10% of the membrane components and mainly exist on the outer surface of the lipid membrane. In the cell membranes of animals, seven main types of sugars, namely D-glucose, D-galactose, D-mannose, L-fucose, N-acetylgalactosamine, and N-acetylglucosamine, are present in the membrane. There are mainly two forms of the binding between sugars and amino acids. N-linkage: The sugar chain binds to the asparagine residue of the peptide chain. O-linkage: The sugar chain binds to the serine or threonine residue of the peptide chain. 4.5 Asymmetry of the Lipid Membrane of Microorganisms There are obvious differences in the components and functions between the inner and outer layers of the lipid membrane, and this difference is called membrane asymmetry. Membrane lipids, membrane proteins, and membrane sugars are all asymmetrically distributed on the membrane. As a result, the asymmetry and directionality of membrane functions occur. That is, due to the different fluidities of the inner and outer layers of the membrane, the movement of substances has a certain directionality, and there are also specific directions in signal reception and transmission, etc. Due to the asymmetry and directionality of membrane functions, the high degree of orderliness of life activities is ensured. Intercellular recognition, movement, substance transport, signal transduction, etc. all have directionality. The maintenance of these directionalties is provided by membrane proteins, membrane lipids, and membrane sugars that are asymmetrically distributed. 4.6 Fluidity of the Lipid Membrane of Microorganisms The lipid membrane of microorganisms has fluidity, and the lipid molecules on the lipid membrane can undergo lateral diffusion, rotation, oscillation, stretching and contraction vibration, inversion, and rotational isomerization. The movement of membrane proteins mainly has two forms: lateral diffusion and rotational diffusion. The fluidity of the lipid membrane is a necessary condition to ensure its normal function. If the fluidity of the lipid membrane is lower than a certain threshold, the activities of many enzymes and transmembrane transport will stop. Conversely, if the fluidity is too high, the dissolution of the lipid membrane will occur.
[0017] 5. Methods for Destroying the Cell Membrane of Microorganisms and Their Formulations 5.1 Physical Damage The simplest method in vitro is to put microorganisms into distilled water, which utilizes the principle of osmosis for cells to absorb water and burst, and can destroy the lipid membrane of microorganisms at both low and high temperatures. Direct differential centrifugation can also destroy the structure of the lipid membrane. 5.2 Destruction by Proteases and Phospholipases Proteases can catalyze the hydrolysis of proteins in the lipid membrane to destroy the lipid membrane, and phospholipases can also destroy the lipid membrane by hydrolyzing phospholipids in the lipid membrane. 5.3 Damage to the Cell Membrane by Ionic, Non-Ionic, and Amphoteric Surfactants Surfactants are amphiphilic molecules that contain both a hydrophilic region and a hydrophobic region, and can disrupt protein, protein-lipid, and lipid bonds, and denature proteins and other macromolecules. Commonly used ionic surfactants in experiments include sodium dodecyl sulfate (SDS), deoxycholate, cholate, sarcosinate, etc. Commonly used non-ionic surfactants include Triton X-100, DDM, digitonin, tween20, tween80, etc. Surfactants are amphiphilic organic compounds composed of a hydrophobic non-polar hydrocarbon moiety and a hydrophilic polar group. This molecular structure closely resembles that of the amphiphilic phospholipids that make up lipid membranes. Phospholipids have hydrophobic tails of two fatty acids, each attached to a hydrophilic group. At high concentrations, amphiphilic molecules self-assemble into a structure that keeps the hydrophilic heads on the outside and the hydrophobic tails on the inside, away from water. Due to differences in molecules, surfactant molecules form spherical micelles. Due to the similarity in molecular structure, surfactants can penetrate lipid bilayers and disrupt lipid membranes. 5.4. In Vitro Bactericidal Action of Fatty Acids Fatty acids are compounds composed of three elements: carbon, hydrogen, and oxygen, and are the main components of neutral fats, phospholipids, and glycolipids. Fatty acids can be classified into short-chain fatty acids, medium-chain fatty acids, and long-chain fatty acids according to the length of the carbon chain. Short-chain fatty acids have less than 6 carbon atoms in the carbon chain and are also called volatile fatty acids. Medium-chain fatty acids are fatty acids with 6 to 12 carbon atoms in the carbon chain. Long-chain fatty acids have more than 12 carbon atoms in the carbon chain. Fatty acids can be classified into three categories: saturated fatty acids, monounsaturated fatty acids, and polyunsaturated fatty acids based on the difference between saturated hydrocarbon chains and unsaturated hydrocarbon chains. That is, saturated fatty acids do not have unsaturated bonds in the hydrocarbon chain. Monounsaturated fatty acids have one unsaturated bond in the hydrocarbon chain. Polyunsaturated fatty acids have two or more unsaturated bonds in the hydrocarbon chain. Fatty acids in food are re-esterified within intestinal cells, mixed with bile salts and monoglycerides to form fat particles of 4 to 6 nm, and these fat particles are directly absorbed by intestinal epithelial cells through phagocytosis, coated on the outside with a membrane of lecithin and protein, becoming chylomicrons, entering the lymphatic system, passing through lymphatic vessels and thoracic ducts, and returning to the bloodstream in the form of an oil-in-water emulsion. Medium-chain fatty acids, except for a small amount that exists in peripheral blood for a short period, mostly non-covalently bind to serum proteins and rapidly reach the liver through the portal system. In the liver, medium-chain fatty acids rapidly pass through the mitochondrial double membrane and are rapidly acylated by the action of octanoyl CoA, but are hardly synthesized into fat. Excess acetyl CoA generated by acylation undergoes various metabolic effects in the cytoplasm of mitochondria, and most of it tends to synthesize ketone bodies. According to research, the antibacterial effects of fatty acids are often extensive. Although their antibacterial mechanisms have not been fully understood, many studies speculate that the main target of the action of fatty acids is the cell membrane, where fatty acids interfere with the electron transport chain and oxidative phosphorylation. In addition to interfering with the energy production of cells, the action of fatty acids can be due to the inhibition of enzyme activity, the impairment of nutrient absorption, the generation of peroxidation and autoxidation decomposition products, or the direct decomposition of bacterial cells. Because its mechanism of action is different from that of most conventional antibiotics, there is a possibility of development. However, many problems have hindered the progress so far. First, some free fatty acids do not taste good. Second, free fatty acids are unstable and tend to bind non-specifically to proteins, and more fatty acids are transported in the body in the form of stable lipids (such as triglycerides). Third, since fatty acids are fat-soluble and have a fast metabolism, they cannot be directly utilized in the body. Free fatty acids are insoluble or have very low solubility in water, so they cannot be directly injected into the bloodstream. Injecting directly into a vein causes pulmonary embolism, and injecting into an artery causes arterial embolism and tissue necrosis. The concentrations of in vitro antibacterial and bactericidal fatty acids used in research are often very high, and such high concentrations will undoubtedly destroy the cell membranes of human cells. Human cells are also composed of phospholipid bilayers and are targeted by the attack of high concentrations of fatty acids. Therefore, the patent of the present invention relates to a group of stable water-soluble carbon chain complexes that can be administered intravenously, intraarterially, or orally. Through hydrophobic carbon chains covalently bonded to large, medium, and small water-soluble molecules and binding molecules, the fat-soluble hydrophobic carbon chains can be converted into water-soluble complexes that can target and kill microorganisms in the body. This group of complexes has the ability to target and kill pathogenic microorganisms at therapeutic concentrations without affecting or damaging human cells and tissues, and can be easily removed by the liver and not metabolized in the short term. The highly water-soluble and highly affinity complexes of the present invention have antibacterial infection effects and can be used not only in nasal sprays and dry powder inhalants but also in intravenous injections and oral dosage forms.
Summary of the Invention
Problems to be Solved by the Invention
[0018] The present invention provides a complex that can prevent, inhibit, or treat microbial infections, addressing the lack of reagents in the prior art that are free of toxicity and side effects and can widely kill, prevent, inhibit, or treat microbial infections.
[0019] In the process of researching substances for preventing, inhibiting, or treating microbial infections, through intensive research, the present inventors found that the water-soluble carbon chain substances of the present invention can affect the structural function of cell membranes and the transmembrane transport of substances. Further research shows that by controlling the specific hydrophilicity and hydrophobicity of the carbon chain substances and / or controlling the concentration of the carbon chain substances as needed, the cell membranes of microorganisms can be destroyed to achieve the effect of preventing, inhibiting, or treating microbial infections. By controlling the concentration within the desired range, it is possible to affect the structure and function of cell membranes and control the transmembrane transport of substances. By controlling the concentration within the desired range, it is also possible to suppress the fluidity of cell membranes and improve the stability of cell membranes, thereby enabling the preparation of anti-aging and anti-inflammatory pharmaceutical preparations according to the place of use.
[0020] The present invention provides a water-soluble carbon chain substance that affects the structural function of cell membranes and the transmembrane transport of substances. That is, according to the research of the present inventors, after the water-soluble carbon chain contacts the cell, the carbon chain portion inserts into the phospholipid bilayer of the cell membrane, changing or affecting the cholesterol, the length, saturation, and arrangement of the fatty acid chains of phospholipid molecules, or changing or affecting the glycerophospholipid / sphingomyelin ratio, thereby changing the structure of the cell membrane. Alternatively, the water-soluble carbon chain binds to membrane proteins, changing or affecting the structure of the membrane proteins, further affecting the structure of the cell membrane. The change in the cell membrane structure changes the asymmetry and directionality of the membrane function, further affecting the directionality of substance transport and signal transduction on the cell membrane, and affecting the transport function of the cell membrane for drug molecules and micronanoparticles.
Means for Solving the Problems
[0021] Specifically, in order to solve the lack of reagents in the prior art that have no toxicity or side effects, especially those that can widely kill, prevent, block, or treat microbial infections, the present invention provides the following first technical solution.
[0022] (1) The present invention provides a complex that can prevent, block, and / or treat microbial infections, comprising an active portion, a binding portion, and a water-soluble portion. The active portion is a lipophilic saturated and / or unsaturated carbon chain having a branched, cyclic structure, and / or a linear structure. The carbon chain is a molecule or a residue of a molecule, and the carbon chain is a carbon chain having 3 to 100 carbon atoms. The water-soluble portion is a molecule or a residue of a molecule that is soluble in water, and the molecule contains one or more functional groups selected from an amide group, a phosphoryloxy group, a carboxylic acid group, a phosphoric acid group, a sulfonic acid group, a sulfonyloxy group, a hydroxy group, a quaternary ammonium group, a thioether group, a disulfide bond, an ether group, a mercapto group, an aldehyde group, an ester group, an amine group, an amino group, a urea group, and a guanidino group. The water-soluble portion may be the one or more functional groups described above that are linked to a carbon chain that is an active portion and / or a linking portion. The linking portion is a molecule or a residue of a molecule that can bind to a microbial lipid membrane, a microbial surface protein, a microbial surface polysaccharide, or a cell wall component, or can bind to a polysaccharide, a protein, or a polypeptide in a microorganism. The linking portion is the same as the water-soluble portion, that is, a protein, a polypeptide, an amino acid, an oligopeptide, an oligosaccharide, a monosaccharide, and / or a polysaccharide molecule or a residue thereof that can bind to a microbial lipid membrane or a surface domain. Here, the number of any one of the active portion, the water-soluble portion, and the linking portion may be one or two or more.
[0023] (2) According to the complex described in Technical Proposal 1, the active portion is a carbon chain or a carbon chain residue having 3 to 100 carbon atoms, preferably 3 to 48 carbon atoms, more preferably 3 to 26 carbon atoms, formed by a substance selected from saturated and / or unsaturated aliphatic hydrocarbons, saturated and / or unsaturated aliphatic alcohols or oxoaliphatic alcohols, saturated and / or unsaturated fatty acids, hydrophobic amino acids, fat-soluble vitamins, steroid lipids, phospholipids, sphingomyelin, glycolipids, and surfactants. Here, preferably, the number of carbon atoms is 3 to 26. The water-soluble portion is a water-soluble molecule or a residue of a molecule containing one or more groups selected from a mercapto group, an amino group, a phosphoric acid group, a carboxylic acid group, a sulfonic acid group, a hydroxy group, an amine group, a urea group, a guanidino group, and a disulfide group. The binding moiety has a group that exerts a binding effect, i.e., it can bind to a microbial lipid membrane, a microbial surface protein, a microbial surface polysaccharide, or a cell wall component, or it can bind to a polysaccharide, protein, or polypeptide in a microorganism. This group is derived from a water-soluble moiety or is derived from one or more groups selected from a mercapto group, an amino group, a phosphate group, a carboxylic acid group, a sulfonic acid group, a hydroxy group, an amine group, a urea group, a guanidino group, and a disulfide group that independently serve as a binding moiety, or it is derived from one or more groups selected from a mercapto group, an amino group, a phosphate group, a carboxylic acid group, a sulfonic acid group, a hydroxy group, an amine group, a urea group, a guanidino group, and a disulfide group that provide a linkage between carbon chains. As a result, the complex has one or more groups selected from a mercapto group, an amino group, a phosphate group, a carboxylic acid group, a sulfonic acid group, a hydroxy group, an amine group, a urea group, a guanidino group, and a disulfide group. That is, for the complex of the present invention, the binding moiety may be the same as the water-soluble moiety, or may simultaneously serve a function of providing a carbon chain of the active moiety.
[0024] Preferably, the binding moiety is one or more selected from a divalent fatty acid or a polyvalent fatty acid, an amino acid, a targeting protein, a targeting polypeptide, and a targeting polysaccharide. More preferably, the complex is a complex formed by linking a fatty acid having 3 to 100 carbon atoms, preferably 3 to 50 carbon atoms, with a water-soluble amino acid, or the complex is a complex formed by linking a fatty acid having 3 to 50 carbon atoms to a targeting polypeptide. Or the complex is a complex formed by reacting a fatty acid having 3 to 100 carbon atoms, preferably 3 to 50 carbon atoms, a targeting polypeptide, and PEG. Alternatively, the complex is a complex formed by reacting a surfactant with one or more selected from divalent fatty acids or polyvalent fatty acids, amino acids, targeting proteins, targeting polypeptides, and targeting polysaccharides. Here, preferably, the surfactant is one or more selected from fatty alcohol polyoxyethylene ethers, fatty acid polyoxyethylene esters, alkyl polyglucosides, fatty acid sucrose esters, sorbitan fatty acid esters, polyoxyethylene sorbitan fatty acid esters, N-fatty acyl-N-methylglucosamine, and mannosylerythritol lipids.
[0025] (3) According to the complex described in Technical Proposal 2, the saturated and / or unsaturated fatty acid is selected from saturated fatty acids or unsaturated fatty acids having 3 to 100 carbon atoms, and the fatty acid is a fatty acid or amino acid containing a double bond, a triple bond, a hydroxy group, an amino group, and / or substituted with oxygen, and may be a monobasic acid, a dibasic acid, or a polybasic acid.
[0026] (4) According to the complex described in Technical Solution 3, the saturated and / or unsaturated fatty acid is one or more selected from saturated fatty acids having 3 to 46 carbon atoms, monoenoic acids having 3 to 34 carbon atoms, dienoic acids having 5 to 30 carbon atoms, trienoic acids having 7 to 30 carbon atoms, tetraenoic acids having 12 to 38 carbon atoms, pentaenoic acids having 12 to 38 carbon atoms, hexaenoic acids having 22 to 38 carbon atoms, acetylenic acids having 6 to 22 carbon atoms, diacetylene acids having 10 to 22 carbon atoms, triacetylene acids having 12 to 22 carbon atoms, enynoic acids having 8 to 20 carbon atoms (preferably acids containing 1 or 2 C=C double bonds and 1 or 2 or 3 triple bonds), fatty acids having a main chain carbon number of 3 to 30 and a branched carbon number of 1 to 10 and / or 1 to 3 hydroxy groups (preferably saturated fatty acids having a methyl group with 1 to 3 carbon atoms or fatty acids having a C=C double bond), saturated linear and branched dicarboxylic acids and tricarboxylic acids having 3 to 38 carbon atoms, unsaturated linear or branched dicarboxylic acids and tricarboxylic acids having 4 to 18 carbon atoms which may be substituted with a hydroxy group, carboxylic acids substituted with an amino group, a hydroxy group, an oxo group and / or a methyl group having 3 to 18 carbon atoms, N-fatty acyl amino acids having 6 to 30 carbon atoms, amino acids containing two or more fatty acyls, and polycarboxylic acids linked by thioether bonds and amide bonds. The saturated and / or unsaturated fatty aliphatic alcohol is a saturated fatty linear or branched alcohol having 3 to 33 carbon atoms, and / or an unsaturated fatty linear or branched alcohol having 3 to 33 carbon atoms and containing 1 to 5 double bonds and 1 to 5 triple bonds and 1 to 3 hydroxy groups. The oxo fatty aliphatic alcohol is an alcohol ketone having 8 to 31 carbon atoms and containing 1 to 3 double bonds or triple bonds and 1 to 3 hydroxy groups, and the ketone is a monoketone or a diketone.
[0027] According to the composite described in Technical Solution 4, the saturated and / or unsaturated fatty acid is one or more selected from fumaric acid, caprylic acid, glutaconic acid, hexanoic acid, nonanoic acid, dodecanoic acid, tetradecanoic acid, hexadecanoic acid, octadecanoic acid, eicosanoic acid, oleic acid, linoleic acid, linolenic acid, eicosapentaenoic acid, docosapentaenoic acid, docosahexaenoic acid, pentacosanoic acid, enanthic acid, decanoic acid, dodecenoic acid, tetradecenoic acid, dotriacontanehexaenoic acid, octacosanoic acid, or a carbon chain residue formed by these.
[0028] (6) According to the composite described in any one of Technical Solutions 1 to 5, the water-soluble part is a molecule or a residue of a molecule containing one or more groups selected from a mercapto group, an amino group, a carboxylic acid group, a hydroxy group, and a disulfide group, and the molecule is one or more water-soluble macromolecules or residues thereof selected from proteins, polysaccharides, nucleic acids, and artificially synthesized water-soluble polymers, and / or one or more medium molecules or residues thereof selected from polypeptides, oligopeptides, oligosaccharides, oligonucleotides, and artificially synthesized medium molecular weight water-soluble polymers, and / or one or more water-soluble small molecules or residues thereof selected from amino acids, monosaccharides, disaccharides, nucleotides, water-soluble vitamins, and deoxyribonucleotides, and / or a molecule or a residue of a molecule linked to the carbon chain that is the active part, and the molecule or the residue of the molecule contains one or more groups selected from a mercapto group, an amino group, a carboxylic acid group, a hydroxy group, and a disulfide group.
[0029] According to the composite described in Technical Solution 6, the protein, which is the water-soluble macromolecule, is one or more water-soluble macromolecules selected from serum albumin, immunoglobulin, water-soluble collagen, chaperone, water-soluble glycoprotein, and CD14; the polysaccharide, which is the macromolecule, is one or more water-soluble macromolecules selected from glucan, hyaluronic acid, sialic acid, heparin sulfate, heparan sulfate, chondroitin sulfate, dermatan sulfate, keratan sulfate, acetylated water-soluble cellulose derivative, β-cyclodextrin and its derivatives, and water-soluble chitosan derivative; the water-soluble polymer, which is the macromolecule, is one or more water-soluble macromolecules selected from polyethylene glycol and carboxylated or aminated polyethylene glycol, polyvinyl alcohol and carboxylated or quaternized polyvinyl alcohol, polyacrylic acid, and ammonium polyacrylate. The medium molecular weight water-soluble polymer is selected from targeting polypeptide, oligopeptide, oligosaccharide, oligonucleotide and / or water-soluble polyamino acid. Preferably, the targeting polypeptide includes specific targeting microbial lipid membrane, cell walls of bacteria and fungi, protein of virus surface protein domain, or neutralizing antibody fragment (including taurine transport peptide, SBP1, etc.). Preferably, the water-soluble polyamino acid is selected from polyglutamic acid, polylysine and / or polyaspartic acid, and oligopeptide, oligosaccharide, oligonucleotide. The water-soluble small molecule monosaccharides and / or disaccharides are one or more selected from glucose, fructose, rhamnose, sorbose, sucrose, maltose, lactose, and trehalose. The water-soluble small molecule nucleotides and / or deoxyribonucleotides are selected from adenylate, guanylate, uridylate, cytidylate, thymidylate, inosine, deoxyadenylate, deoxyguanylate, deoxycytidylate, and deoxythymidylate. The amino acids that are the water-soluble small molecules are one or more selected from serine, threonine, cysteine, asparagine, glutamine, tyrosine, lysine, arginine, histidine, aspartic acid, glutamic acid, citrulline, ornithine, taurine, and aminobutyric acid. The vitamins that are the water-soluble small molecules are one or more selected from vitamin B1, pantothenic acid, vitamin B6, and vitamin C.
[0030] (8) According to the complex described in any one of Technical Solutions 1 to 7, the binding moiety is the same as the water-soluble moiety, that is, a microbial lipid membrane, a protein, polypeptide, oligopeptide, oligosaccharide, monosaccharide, disaccharide, amino acid, nucleotide, vitamin, water-soluble polymer, water-soluble polyamino acid and / or polysaccharide molecule or a residue of these molecules that can bind to the surface domain. The molecule or the residue of the molecule contains one or more groups selected from a mercapto group, an amino group, a carboxylic acid group, a hydroxy group, and a disulfide group.
[0031] According to the complex of any one of (9) Technical Solutions 1 to 8, it is a compound obtained by reacting a substance containing a carbon chain having 3 to 100 carbon atoms as an active moiety with one or more selected from proteins, polypeptides, oligopeptides, oligosaccharides, monosaccharides, disaccharides, amino acids, nucleotides, vitamins, water-soluble polymers, water-soluble polyamino acids, and / or polysaccharides, or a compound obtained by reacting a substance containing a carbon chain having 3 to 100 carbon atoms as an active moiety with one or more selected from protein, polypeptide, oligopeptide, oligosaccharide, monosaccharide, disaccharide, amino acid, nucleotide, vitamin, water-soluble polymer, water-soluble polyamino acid, and / or polysaccharide molecules, and a mixture of the unreacted substance of the active moiety and / or the unreacted protein, polypeptide, oligopeptide, oligosaccharide, monosaccharide, disaccharide, amino acid, nucleotide, vitamin, water-soluble polymer, water-soluble polyamino acid, and / or polysaccharide molecules. Here, preferably, the substance of the active moiety is one or more substances selected from saturated and / or unsaturated aliphatic hydrocarbons, saturated and / or unsaturated aliphatic alcohols or oxoaliphatic alcohols, saturated and / or unsaturated fatty acids, hydrophobic amino acids, fat-soluble vitamins, steroid lipids, phospholipids, sphingomyelin, glycolipids, and surfactants, and these substances provide or have a carbon chain having 3 to 100 carbon atoms, preferably 3 to 48 carbon atoms, more preferably 3 to 26 carbon atoms or a residue forming a carbon chain.
[0032] That is, the related complex for preventing, arresting, or treating microbial infection includes the compound obtained by the reaction, and also includes the reaction mixture containing the compound obtained by the reaction (also referred to as "reaction product", or "reaction mixture", "reaction product solution", "reaction mixture solution"), and the purified product after purifying the reaction mixture to separate unreacted reaction starting materials, catalysts, etc.
[0033] According to the composite of any one of Technical Solutions 1 to 8, it is a composite obtained by complexing a substance containing a carbon chain having 3 to 100 carbon atoms as an active moiety with one or more selected from proteins, polypeptides, oligopeptides, oligosaccharides, monosaccharides, disaccharides, amino acids, nucleotides, vitamins, water-soluble polymers, water-soluble polyamino acids, and / or polysaccharide molecules by physicochemical action, or a mixture directly physically mixed, wherein the physicochemical action includes hydrogen bonding or van der Waals force or a combination of both of these actions. Here, preferably, the substance that is the active moiety is one or more substances selected from saturated and / or unsaturated aliphatic hydrocarbons, saturated and / or unsaturated aliphatic alcohols or oxoaliphatic alcohols, saturated and / or unsaturated fatty acids, hydrophobic amino acids, fat-soluble vitamins, steroid lipids, phospholipids, sphingomyelin, glycolipids, and surfactants, and these substances provide or have a carbon chain having 3 to 100 carbon atoms, preferably 3 to 48 carbon atoms, more preferably 3 to 26 carbon atoms or a residue forming a carbon chain.
[0034] (11) According to the composite of Technical Solution 9, it is a compound obtained by reacting a substance containing a carbon chain having 3 to 100 carbon atoms as an active moiety with at least one selected from proteins, polypeptides, oligopeptides, and amino acids, or a mixture of a compound obtained by reacting a substance having a carbon chain having 3 to 100 carbon atoms as an active moiety with at least one selected from proteins, polypeptides, oligopeptides, and amino acids, and at least one selected from the unreacted substance that is the active moiety and / or the unreacted proteins, polypeptides, oligopeptides, and amino acids.
[0035] According to the complex described in Technical Proposal 9, it is a compound obtained by reacting a substance containing a carbon chain with 3 to 100 carbon atoms as an active moiety, PEG, and at least one selected from proteins, polypeptides, oligopeptides, and amino acids, or a compound obtained by reacting a substance having a carbon chain with 3 to 100 carbon atoms as an active moiety, PEG, and at least one selected from proteins, polypeptides, oligopeptides, and amino acids, and a mixture of the unreacted substance of the active moiety, unreacted PEG, and / or at least one selected from unreacted proteins, polypeptides, oligopeptides, and amino acids.
[0036] (13) According to the complex described in Technical Proposal 9, it is a compound obtained by reacting a substance containing a carbon chain with 3 to 100 carbon atoms as an active moiety with one or more selected from polysaccharides, monosaccharides, disaccharides, and / or oligosaccharides, or a compound obtained by reacting a substance having a carbon chain with 3 to 100 carbon atoms as an active moiety with one or more selected from polysaccharides, monosaccharides, disaccharides, and / or oligosaccharides, and a mixture of the unreacted substance of the active moiety and / or unreacted polysaccharides, monosaccharides, disaccharides, and / or oligosaccharides.
[0037] (14) According to the complex described in Technical Proposal 9, it is a compound obtained by reacting a substance containing a carbon chain with 3 to 100 carbon atoms as an active moiety, PEG, and one or more selected from polysaccharides, monosaccharides, disaccharides, and / or oligosaccharides, or a compound obtained by reacting saturated and / or unsaturated fatty acids with 3 to 100 carbon atoms, PEG, and one or more selected from polysaccharides, monosaccharides, disaccharides, and / or oligosaccharides, and a mixture of the unreacted substance of the active moiety, unreacted PEG, and / or unreacted polysaccharides, monosaccharides, disaccharides, and / or oligosaccharides.
[0038] (15) According to the complex described in any one of Technical Proposals 6 to 12, the protein is one or more selected from serum albumin, immunoglobulin, water-soluble collagen, chaperone, water-soluble glycoprotein, and CD14.
[0039] (16) According to the complex described in Technical Solution 13, the polysaccharide is one or more selected from glucan and / or hyaluronic acid sialic acid, heparin sulfate, heparan sulfate, chondroitin sulfate, dermatan sulfate, keratan sulfate, acetylated water-soluble cellulose derivatives, β-cyclodextrin and its derivatives, and water-soluble chitosan derivatives.
[0040] (17) According to the complex described in Technical Solution 11 or 12, it is a compound obtained by reacting a substance containing a carbon chain of 3 to 100 carbon atoms as an active moiety, a linker, and a protein containing a mercapto group, or a mixture of a compound obtained by the above reaction, the substance that is the unreacted active moiety, the unreacted linker, and / or the protein containing an unreacted mercapto group. Here, the linker is one or more of amino acids, succinic acid, butadienoic acid, glutaconic acid, hexamiminodiacid, urethane, short peptides, N-hydroxybutenimide, polyethylene glycol, and derivatives of the above compounds. Preferably, the complex is a compound obtained by reacting a substance containing a carbon chain of 3 to 100 carbon atoms as an active moiety, N-hydroxybutenimide, and a protein containing a mercapto group, or a mixture of a compound obtained by the above reaction, the substance that is the unreacted active moiety, the unreacted N-hydroxybutenimide, and / or the protein containing an unreacted mercapto group.
[0041] (18) According to the complex described in Technical Solution 13, it is a compound obtained by reacting a substance containing a carbon chain of 3 to 100 carbon atoms as an active moiety, cystamine, and one or more selected from polysaccharides, monosaccharides, disaccharides, and / or oligosaccharides, or a mixture of a compound obtained by reacting a substance containing a carbon chain of 3 to 100 carbon atoms as an active moiety, cystamine, and one or more selected from polysaccharides, monosaccharides, disaccharides, and / or oligosaccharides, the substance that is the unreacted active moiety, the unreacted polysaccharides, monosaccharides, disaccharides, oligosaccharides, and / or the unreacted cystamine.
[0042] According to the complex according to any one of Technical Solutions 8 to 17, the compound obtained by the reaction contains one or more of an amide group, an ester group, a thioether group, or an ether group as a linking portion between the water-soluble portion and the functional portion.
[0043] (20) According to the complex according to any one of Technical Solutions 3 to 18, the substance that provides a carbon chain or a residue of a carbon chain as the functional portion is a saturated and / or unsaturated aliphatic hydrocarbon, a saturated and / or unsaturated aliphatic alcohol or an oxoaliphatic alcohol, a saturated and / or unsaturated fatty acid, a hydrophobic amino acid, a fat-soluble vitamin, a steroid lipid, a phospholipid, sphingomyelin, a glycolipid, and a surfactant, and is one or more selected therefrom, and the carbon chain has 3 to 100 carbon atoms, preferably 3 to 50 carbon atoms, more preferably 3 to 48 carbon atoms, and even more preferably 3 to 26 carbon atoms.
[0044] (21) According to the complex according to any one of Technical Solutions 3 to 18, the substance that provides a carbon chain or a residue of a carbon chain as the functional portion is a saturated and / or unsaturated aliphatic hydrocarbon, a saturated and / or unsaturated aliphatic alcohol or an oxoaliphatic alcohol, a saturated and / or unsaturated fatty acid, a hydrophobic amino acid, a fat-soluble vitamin, a steroid lipid, a phospholipid, sphingomyelin, a glycolipid, and a surfactant, and is one or more selected therefrom, preferably a saturated and / or unsaturated fatty acid, and more preferably the saturated and / or unsaturated fatty acid is a fatty acid containing 1 to 8 C=C double bonds having 3 to 100 carbon atoms, preferably 3 to 50 carbon atoms, more preferably 3 to 48 carbon atoms, and even more preferably 3 to 40 carbon atoms, and may be a fatty acid containing 1 to 7 C=C double bonds, a fatty acid containing 1 to 6 double bonds, a fatty acid containing 1 to 5 double bonds, a fatty acid containing 1 to 4 double bonds, a fatty acid containing 1 to 3 double bonds, or a fatty acid containing 1 to 2 double bonds.
[0045] According to the complex described in any one of Technical Solutions 3 to 18, the substance providing a carbon chain or a residue of a carbon chain as the functional part is a saturated and / or unsaturated fatty acid, which may be a fatty acid containing 1 to 6 double bonds and having 2 to 30 carbon atoms, preferably 2 to 26 carbon atoms, more preferably 2 to 22 carbon atoms.
[0046] (23) According to the complex described in any one of Technical Solutions 3 to 18, the saturated and / or unsaturated fatty acid has 3 to 30 carbon atoms, preferably 3 to 26 carbon atoms, preferably 8 to 22 carbon atoms, preferably 8 to 20 carbon atoms, preferably 8 to 18 carbon atoms.
[0047] (24) According to the complex described in any one of Technical Solutions 3 to 18, the saturated and / or unsaturated fatty acid is one or more fatty acids selected from fumaric acid, caprylic acid, glutaconic acid, hexanoic acid, nonanoic acid, dodecanoic acid, tetradecanoic acid, hexadecanoic acid, octadecanoic acid, eicosanoic acid, oleic acid, linoleic acid, linolenic acid, eicosapentaenoic acid, docosapentaenoic acid, docosahexaenoic acid, pentacosanic acid, enanthic acid, decanoic acid, dodecenoic acid, tetradecenoic acid, dotriacontanehexaenoic acid, octacosanoic acid.
[0048] (25) According to the complex described in any one of Technical Solutions 8 to 23, the protein is human serum protein or bovine serum protein, or CD14, or the polysaccharide is glucan and / or hyaluronic acid.
[0049] (26) According to the complex described in Technical Solution 11, the compound obtained by the reaction is one or more compounds having the following structural formula obtained by reacting a fatty acid with albumin or SBP1.
Chemical formula
[0050] According to the composite described in Technical Solution 12, the compound obtained by the reaction is a compound obtained by reacting a monovalent fatty acid having 3 to 10 carbon atoms, PEG, and an amino acid, or a compound obtained by reacting a monovalent fatty acid having 3 to 10 carbon atoms, a saturated divalent fatty acid having 5 to 8 carbon atoms, PEG, and taurine, and is preferably a compound having at least one of the following structural formulas.
Chemical formula
[0051] (28) According to the composite described in Technical Solution 13, the compound obtained by the reaction is any one or more compounds having the following structural formulas obtained by reacting a fatty acid and glucan.
Chemical formula
[0052] (29) According to the composite described in Technical Solution 13, the compound obtained by the reaction is any one or more compounds having the following structural formulas obtained by reacting a fatty acid and hyaluronic acid.
Chemical formula
Chemical formula
[0053] (30) According to the composite described in Technical Solution 14, the compound obtained by the reaction is a compound obtained by reacting a fatty acid having 3 to 10 carbon atoms, PEG, and glucose, and is preferably a compound having the following structural formula.
Chemical formula
[0054] According to the composite described in Technical Proposal 17, the compound obtained by the reaction is any one or more compounds having a thioether bond and having the following structural formula, which are obtained by reacting a fatty acid, N-hydroxybutanimide, and albumin.
Chemical formula
Chemical formula
Chemical formula
[0055] (32) According to the composite described in Technical Proposal 18, the compound obtained by the reaction is any one or more compounds having the following structural formula, which are obtained by reacting a fatty acid, cystamine, and glucan.
Chemical formula
[0056] According to the composite described in Technical Solution 18, the compound obtained by the reaction is any one or more compounds having the following structural formula, which are obtained by reacting a fatty acid, cystamine, and hyaluronic acid.
Chemical formula
[0057] (34) According to the composite described in any one of Technical Proposals 1 to 8, it is a compound obtained by reacting a surfactant containing a carbon chain having 3 to 30 carbon atoms with a divalent fatty acid or polyvalent fatty acid, an amino acid, a targeting protein, a targeting polypeptide, a targeting polysaccharide and / or a targeting polysaccharide, or a mixture of the compound obtained by the above reaction with the unreacted surfactant and / or the unreacted divalent fatty acid or polyvalent fatty acid, amino acid, targeting protein, targeting polypeptide, targeting polysaccharide and / or targeting polysaccharide.
[0058] (35) According to the complex described in Technical Solution 34, the surfactant is one or more selected from fatty alcohol polyoxyethylene ether, fatty acid polyoxyethylene ester, alkyl polyglucoside, sucrose fatty acid ester, sorbitan fatty acid ester, polyoxyethylene sorbitan fatty acid ester, mannosylerythritol lipid, and N-fatty acyl-N-methylglucosamine.
[0059] (36) According to the complex described in any one of Technical Solutions 1 to 35, the microbial infection includes an infection caused by a virus.
[0060] (37) A preparation for preventing, inhibiting or treating a microbial infection prepared using the complex described in any one of Technical Solutions 1 to 35.
[0061] (38) According to the preparation described in Technical Solution 37, the preparation is a pharmaceutical preparation or an environmental disinfection and sterilization preparation.
[0062] (39) According to the preparation described in Technical Solution 38, the pharmaceutical preparation is one selected from an inhalant, a nasal spray, an injection, an oral preparation, and a topical skin dosage form.
[0063] (40) Use of the complex described in any one of Technical Solutions 1 to 35 in the preparation of a pharmaceutical preparation for preventing, inhibiting and / or treating a microbial infection.
[0064] (41) According to the use described in Technical Solution 40, the microbe is any one or more selected from a virus, a bacterium, a fungus, Chlamydia or Mycoplasma.
[0065] (42) According to the use described in Technical Solution 41, the virus is an enveloped virus and / or a non-enveloped virus.
[0066] According to the use described in Technical Solution 42, the enveloped virus is one or more of coronavirus, influenza virus, human immunodeficiency virus, hepatitis B virus, hepatitis C virus, herpes virus, Zika virus, dengue virus, Japanese encephalitis virus, Ebola virus, rabies virus, and / or hantavirus, and the non-enveloped virus is two or more of hepatitis A virus, human papillomavirus, poliovirus and / or coxsackievirus.
[0067] (44) According to the use described in Technical Solution 43, the virus is any one or more of coronavirus, human immunodeficiency virus, hepatitis B virus, hepatitis C virus, herpes virus, Japanese encephalitis virus, rabies virus, human papillomavirus and Ebola virus.
[0068] (45) According to the use described in Technical Solution 41, the bacterium is a Gram-positive bacterium and / or a Gram-negative bacterium, the fungus is a pathogenic fungus and / or a conditional pathogenic fungus, the Chlamydia is Chlamydia trachomatis, Chlamydia pneumoniae and / or Chlamydia psittaci, and the Mycoplasma includes Mycoplasma pneumoniae, Mycoplasma ureaplasma, Mycoplasma hominis, and / or Mycoplasma genitalium.
[0069] (46) According to the use described in Technical Solution 41, the bacterium is one or more selected from Escherichia coli, Staphylococcus aureus, methicillin-resistant Staphylococcus aureus, Streptococcus pneumoniae, Klebsiella pneumoniae, and Pseudomonas aeruginosa, and the fungus is one or more selected from Candida albicans, Aspergillus niger, anaerobic positive bacilli, ascomycetes, Aspergillus proteus, and Microsporum canis.
[0070] (47) According to the use described in Technical Solution 41, the virus is one or more selected from H7N9 influenza virus, H5N1 influenza virus, HIV virus, novel coronavirus, HPV virus and rabies virus.
[0071] (48) A compound having a lipophilic saturated and / or unsaturated carbon chain with a branched, cyclic structure and / or linear structure, a water-soluble molecule, a protein, polypeptide, amino acid, oligopeptide, oligosaccharide, monosaccharide and / or polysaccharide molecule that can bind to a microbial lipid membrane, viral surface domain or cell wall, which may be added as required, and a linker molecule that may be added as required are reacted in the presence of a catalyst to obtain the complex, which is the method for preparing the complex according to any one of Technical Solutions 1 to 35.
[0072] (49) According to the method for preparing the complex described in Technical Solution 48, the complex is a product obtained by purifying the compound obtained by the reaction.
[0073] (50) A compound having a lipophilic saturated and / or unsaturated carbon chain with a branched, cyclic structure and / or linear structure, a water-soluble molecule, and a protein, polypeptide, amino acid, oligopeptide, oligosaccharide, monosaccharide and / or polysaccharide molecule that can bind to a microbial lipid membrane, microbial surface domain or cell wall, which may be added as required, are physically mixed to obtain the complex, which is the method for preparing the complex according to any one of Technical Solutions 1 to 35.
[0074] (51) A saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms and any one substance of protein, polypeptide, oligopeptide, oligosaccharide, monosaccharide, disaccharide, nucleotide, vitamin, water-soluble polymer, water-soluble polyamino acid and / or polysaccharide are reacted in the presence of a catalyst to obtain the complex, which is the method for preparing the complex according to any one of Technical Solutions 1 to 35.
[0075] (52) According to the method for preparing the complex described in Technical Solution 51, the complex is a product obtained by purifying the compound obtained by the reaction.
[0076] (53) A method for preparing a complex according to any one of Technical Solutions 1 to 35, which comprises complexing a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms with a protein, polypeptide, oligopeptide, oligosaccharide, monosaccharide, disaccharide, nucleotide, vitamin, water-soluble polymer, water-soluble polyamino acid and / or polysaccharide molecule by physicochemical action to obtain a complex, or directly physically mixing them to obtain the complex.
[0077] Specifically, in order to solve the lack of reagents that have no toxicity and side effects in the prior art and can widely kill, prevent, block or treat microbial infections, the present invention provides the following second technical solution.
[0078] (1) A complex capable of preventing, blocking and / or treating microbial infections, comprising an active part, a binding part and a water-soluble part. The active part is a lipophilic saturated and / or unsaturated carbon chain having a branched, cyclic structure and / or a linear structure, and the carbon chain is a molecule or a residue of a molecule. Here, the active part is a hydrophobic amino acid, a fat-soluble vitamin, a steroid lipid, a phospholipid, sphingomyelin, a glycolipid, a surfactant, a saturated and / or unsaturated aliphatic hydrocarbon and a saturated and / or unsaturated aliphatic alcohol or an oxoaliphatic alcohol, and is a carbon chain or a residue of a carbon chain having 3 to 100 carbon atoms formed by one or more substances selected therefrom. The water-soluble part is a molecule or a residue of a molecule soluble in water, and the molecule contains one or more functional groups selected from an amide group, a phosphoryloxy group, a carboxylic acid group, a phosphate group, a sulfonic acid group, a sulfonyloxy group, a hydroxy group, a quaternary ammonium group, a thioether group, a disulfide bond, an ether group, a mercapto group, an aldehyde group, an ester group, an amine group, an amino group, a urea group and a guanidino group. The water-soluble part may be one or more of the above functional groups linked to the carbon chain which is the active part. The binding moiety is a molecule or a residue of a molecule that can bind to a microbial lipid membrane, a microbial surface protein, a microbial surface polysaccharide, or a cell wall component, or can bind to a polysaccharide, protein, or polypeptide in a microorganism. The binding moiety is the same as the water-soluble moiety, i.e., it may be a protein, polypeptide, amino acid, oligopeptide, oligosaccharide, monosaccharide, and / or polysaccharide molecule or a residue thereof that can bind to a microbial lipid membrane or a surface domain. Here, the number of any one of the active moiety, the water-soluble moiety, and the binding moiety may be one or two or more.
[0079] (2) According to the complex described in Technical Solution 1, the number of carbon atoms is from 3 to 48.
[0080] (3) According to the complex described in Technical Solution 1, the number of carbon atoms is from 3 to 26.
[0081] (4) According to the complex described in any one of Technical Solutions 1 to 3, the water-soluble moiety is a water-soluble molecule or a residue of a molecule containing one or more groups selected from a mercapto group, an amino group, a phosphate group, a carboxylic acid group, a sulfonic acid group, a hydroxy group, an amine group, a urea group, a guanidino group, and a disulfide group. The binding moiety has a group that exerts a binding effect, that is, it can bind to a microbial lipid membrane, a microbial surface protein, a microbial surface polysaccharide, or a cell wall component, or can bind to a polysaccharide, protein, or polypeptide in a microorganism. This group is derived from a water-soluble moiety or is derived from two or more groups selected from a mercapto group, an amino group, a phosphate group, a carboxylic acid group, a sulfonic acid group, a hydroxy group, an amine group, a urea group, a guanidino group, and a disulfide group that independently serve as a binding moiety, or is derived from one or two or more groups selected from a mercapto group, an amino group, a phosphate group, a carboxylic acid group, a sulfonic acid group, a hydroxy group, an amine group, a urea group, a guanidino group, and a disulfide group that provide a linkage between carbon chains. Thereby, the complex has one or two or more groups among a mercapto group, an amino group, a phosphate group, a carboxylic acid group, a sulfonic acid group, a hydroxy group, an amine group, a urea group, a guanidino group, and a disulfide group.
[0082] (5) According to the complex described in Technical Proposal 4, the binding moiety is one or two or more selected from a divalent fatty acid or a polyvalent fatty acid, an amino acid, a targeting protein, a targeting polypeptide, and a targeting polysaccharide.
[0083] (6) According to the complex described in any one of Technical Proposals 1 to 4, the complex is a complex formed by reacting a surfactant with one or two or more selected from a divalent fatty acid or a polyvalent fatty acid, an amino acid, a targeting protein, a targeting polypeptide, and a targeting polysaccharide.
[0084] According to the composite of any one of Technical Solutions 1 to 6, the saturated and / or unsaturated aliphatic alcohol is a saturated alicyclic structure, linear or branched alcohol having 3 to 33 carbon atoms, and / or an unsaturated aliphatic linear or branched alcohol containing 1 to 5 double bonds and 1 to 5 triple bonds having 3 to 33 carbon atoms and containing 1 to 3 hydroxy groups, the oxoaliphatic alcohol is an alcohol ketone containing 1 to 3 double bonds or triple bonds having 8 to 31 carbon atoms and containing 1 to 3 hydroxy groups, and the ketone is a monoketone or diketone.
[0085] (8) According to the composite of any one of Technical Solutions 1 to 5 and Technical Solution 7, the water-soluble part is a molecule or a residue of a molecule containing one or more groups selected from a mercapto group, an amino group, a carboxylic acid group, a hydroxy group, and a disulfide group, and the molecule is one or more water-soluble macromolecules or residues thereof selected from proteins, polysaccharides, nucleic acids, and artificially synthesized water-soluble polymers, and / or one or more medium molecules or residues thereof selected from polypeptides, oligopeptides, oligosaccharides, oligonucleotides, and artificially synthesized medium molecular weight water-soluble polymers, and / or one or more water-soluble small molecules or residues thereof selected from amino acids, monosaccharides, disaccharides, nucleotides, water-soluble vitamins, and deoxyribonucleotides, and / or a molecule or a residue of a molecule linked to the carbon chain which is the active part, and the molecule or the residue of the molecule contains one or more groups selected from a mercapto group, an amino group, a carboxylic acid group, a hydroxy group, and a disulfide group.
[0086] According to the composite described in Technical Solution 8, the protein, which is the water-soluble macromolecule, is one or more water-soluble macromolecules selected from serum albumin, immunoglobulin, water-soluble collagen, chaperone, water-soluble glycoprotein, and CD14; the polysaccharide, which is the macromolecule, is one or more water-soluble macromolecules selected from glucan, hyaluronic acid, sialic acid, heparin sulfate, heparan sulfate, chondroitin sulfate, dermatan sulfate, keratan sulfate, acetylated water-soluble cellulose derivative, β-cyclodextrin and its derivatives, and water-soluble chitosan derivative; the water-soluble polymer, which is the macromolecule, is one or more water-soluble macromolecules selected from polyethylene glycol and carboxylated or aminated polyethylene glycol, polyvinyl alcohol and carboxylated or quaternized polyvinyl alcohol, polyacrylic acid, and ammonium polyacrylate. The medium molecular weight water-soluble polymer is one or more substances selected from targeting polypeptide, oligopeptide, oligosaccharide, oligonucleotide, and / or water-soluble polyamino acid. The water-soluble small molecule monosaccharide and / or disaccharide is one or more selected from glucose, fructose, rhamnose, sorbose, sucrose, maltose, lactose, and trehalose; the nucleotide and / or deoxyribonucleotide, which is the water-soluble small molecule, is selected from adenylate, guanylate, uridylate, cytidylate, thymidylate, inosine, deoxyadenylate, deoxyguanylate, deoxycytidylate, deoxythymidylate; the amino acid, which is the water-soluble small molecule, is one or more selected from serine, threonine, cysteine, asparagine, glutamine, tyrosine, lysine, arginine, histidine, aspartic acid, glutamic acid, citrulline, ornithine, taurine, and aminobutyric acid; the vitamin, which is the water-soluble small molecule, is one or more selected from vitamin B1, pantothenic acid, vitamin B6, and vitamin C.
[0087] According to the complex described in any one of Technical Solutions 5 to 9, the targeting polypeptide includes any one of a specific targeting microbial lipid membrane, the cell walls of bacteria and fungi, the protein of a viral surface protein domain, or a neutralizing antibody fragment.
[0088] (11) According to the complex described in Technical Solution 9, the water-soluble polyamino acid is selected from polyglutamic acid, polylysine and / or polyaspartic acid.
[0089] (12) According to the complex described in any one of Technical Solutions 1 to 11, the binding moiety is the same as the water-soluble moiety, that is, a microbial lipid membrane, a protein, polypeptide, oligopeptide, oligosaccharide, monosaccharide, disaccharide, amino acid, nucleotide, vitamin, water-soluble polymer, water-soluble polyamino acid and / or a polysaccharide molecule or a residue of these molecules that can bind to the surface domain, and the molecule or residue of the molecule contains one or more groups selected from a mercapto group, an amino group, a carboxylic acid group, a hydroxy group, and a disulfide group.
[0090] (13) According to the complex described in Technical Solutions 1 to 12, it is a compound obtained by reacting a substance containing a carbon chain having 3 to 100 carbon atoms as an active moiety with any one or more selected from proteins, polypeptides, oligopeptides, oligosaccharides, amino acids, monosaccharides, disaccharides, nucleotides, vitamins, water-soluble polymers, water-soluble polyamino acids and / or polysaccharide molecules, or a compound obtained by reacting a substance containing a carbon chain having 3 to 100 carbon atoms as an active moiety with any one or more selected from proteins, polypeptides, oligopeptides, oligosaccharides, amino acids, monosaccharides, disaccharides, nucleotides, vitamins, water-soluble polymers, water-soluble polyamino acids and / or polysaccharide molecules, and a mixture of the unreacted substance of the active moiety and / or the unreacted protein, polypeptide, oligopeptide, oligosaccharide, amino acid, monosaccharide, disaccharide, oligonucleotide, vitamin, water-soluble polymer, water-soluble polyamino acid and / or polysaccharide molecule, Here, the substance containing a carbon chain having 3 to 100 carbon atoms as an active moiety is a substance selected from saturated and / or unsaturated aliphatic hydrocarbons, saturated and / or unsaturated aliphatic alcohols or oxoaliphatic alcohols, hydrophobic amino acids, fat-soluble vitamins, steroid lipids, phospholipids, sphingomyelin, glycolipids, and / or surfactants.
[0091] (14) According to the complex described in any one of Technical Solutions 1 to 12, it is a complex obtained by complexing a substance containing a carbon chain having 3 to 100 carbon atoms as an active moiety and any one or two selected from proteins, polypeptides, oligopeptides, oligosaccharides, amino acids, monosaccharides, disaccharides, nucleotides, vitamins, water-soluble polymers, water-soluble polyamino acids, and polysaccharide molecules by physicochemical action, or a mixture directly physically mixed, and the physicochemical action includes hydrogen bonding or van der Waals forces or a combination of both of these actions. Here, the substance containing a carbon chain having 3 to 100 carbon atoms as an active moiety is a substance selected from saturated and / or unsaturated aliphatic hydrocarbons, saturated and / or unsaturated aliphatic alcohols or oxoaliphatic alcohols, hydrophobic amino acids, fat-soluble vitamins, steroid lipids, phospholipids, sphingomyelin, glycolipids, and / or surfactants.
[0092] (15) According to the complex described in Technical Solution 13, it is a compound obtained by reacting a substance containing a carbon chain having 3 to 100 carbon atoms as an active moiety and at least one selected from proteins, polypeptides, oligopeptides, and amino acids, or a compound obtained by reacting a substance containing a carbon chain having 3 to 100 carbon atoms as an active moiety and at least one selected from proteins, polypeptides, oligopeptides, and amino acids, and a mixture of the unreacted substance of the active moiety and / or at least one selected from the unreacted proteins, polypeptides, oligopeptides, and amino acids.
[0093] (16) According to the complex described in Technical Proposal 13, it is a compound obtained by reacting a substance containing a carbon chain having 3 to 100 carbon atoms as an active moiety, PEG, and at least one selected from proteins, polypeptides, oligopeptides, and amino acids, or a mixture of a compound obtained by reacting a substance containing a carbon chain having 3 to 100 carbon atoms as an active moiety, PEG, and at least one selected from proteins, polypeptides, oligopeptides, and amino acids, and a substance which is the unreacted active moiety, unreacted PEG and / or at least one selected from unreacted proteins, polypeptides, oligopeptides, and amino acids.
[0094] (17) According to the complex described in Technical Proposal 13, it is a compound obtained by reacting a substance containing a carbon chain having 3 to 100 carbon atoms as an active moiety with at least one selected from polysaccharides, monosaccharides, disaccharides, and oligosaccharides, or a mixture of a compound obtained by reacting a substance containing a carbon chain having 3 to 100 carbon atoms as an active moiety with at least one selected from polysaccharides, monosaccharides, disaccharides, and oligosaccharides, and a substance which is the unreacted active moiety and / or unreacted polysaccharides, monosaccharides, disaccharides and / or oligosaccharides.
[0095] (18) According to the complex described in Technical Proposal 13, it is a compound obtained by reacting a substance containing a carbon chain having 3 to 100 carbon atoms as an active moiety, PEG, and at least one selected from polysaccharides, monosaccharides, disaccharides, and oligosaccharides, or a mixture of a compound obtained by reacting a substance containing a carbon chain having 3 to 100 carbon atoms as an active moiety, PEG, and at least one selected from polysaccharides, monosaccharides, disaccharides, and oligosaccharides, and a substance which is the unreacted active moiety, unreacted PEG and / or unreacted polysaccharides, monosaccharides, disaccharides and / or oligosaccharides.
[0096] (19) According to the complex described in Technical Proposal 13, the protein is one or more selected from serum albumin, immunoglobulin, water-soluble collagen, chaperone, water-soluble glycoprotein, and CD14.
[0097] (20) According to the composite body described in any one of Technical Proposals 13 to 19, the polysaccharide is one or more selected from glucan and / or hyaluronic acid, sialic acid, heparin sulfate, heparan sulfate, chondroitin sulfate, dermatan sulfate, keratan sulfate, acetylated water-soluble cellulose derivative, β-cyclodextrin and its derivatives, and water-soluble chitosan derivatives.
[0098] (21) According to the composite body described in Technical Proposal 13, it is a compound obtained by reacting a substance containing a carbon chain having 3 to 100 carbon atoms as an active portion, a linker, and a protein containing a mercapto group, or a mixture of a compound obtained by the above reaction, the substance that is the unreacted active portion, the unreacted linker, and / or the protein containing the unreacted mercapto group. Here, the linker is one or more of amino acid, succinic acid, butadienoic acid, glutaconic acid, hexamiminodiacid, urethane, short peptide, N-hydroxybutenimide, polyethylene glycol, and derivatives of the above compounds.
[0099] (22) According to the composite body described in Technical Proposal 21, the composite body is a compound obtained by reacting a substance containing a carbon chain having 3 to 100 carbon atoms as an active portion, N-hydroxybutenimide, and a protein containing a mercapto group, or a mixture of a compound obtained by the above reaction, the substance that is the unreacted active portion, the unreacted N-hydroxybutenimide and / or the protein containing the unreacted mercapto group.
[0100] (23) According to the composite body described in Technical Proposal 13, it is a compound obtained by reacting a substance containing a carbon chain having 3 to 100 carbon atoms as an active portion, cystamine, and at least one selected from polysaccharides, monosaccharides, disaccharides, and oligosaccharides, or a compound obtained by reacting a substance containing a carbon chain having 3 to 50 carbon atoms as an active portion, cystamine, and at least one selected from polysaccharides, monosaccharides, disaccharides, and oligosaccharides, and a mixture of the unreacted substance that is the active portion, the unreacted polysaccharides, monosaccharides, disaccharides, oligosaccharides and / or the unreacted cystamine.
[0101] (24) According to the complex described in any one of Technical Solutions 13 to 23, the compound obtained by the reaction contains one or more of an amide group, an ester group, a thioether group, or an ether group as a linking moiety between the water-soluble moiety and the functional moiety.
[0102] (25) According to the complex described in any one of Technical Solutions 4 to 23, the saturated and / or unsaturated aliphatic hydrocarbon, saturated and / or unsaturated aliphatic alcohol, or oxoaliphatic alcohol has 3 to 50 carbon atoms.
[0103] (26) According to the complex described in Technical Solution 25, the number of carbon atoms is 3 to 48.
[0104] (27) According to the complex described in Technical Solution 26, the number of carbon atoms is 3 to 26.
[0105] (28) According to the complex described in any one of Technical Solutions 4 to 23, the protein is human serum protein or bovine serum protein, or CD14, or the polysaccharide is glucan, heparin, and / or hyaluronic acid.
[0106] (29) According to the complex described in any one of Technical Solutions 4 to 12, it is a compound obtained by reacting a surfactant containing a carbon chain having 3 to 30 carbon atoms with at least one selected from a divalent fatty acid or polyvalent fatty acid, an amino acid, a targeting protein, a targeting polypeptide, and a targeting polysaccharide, or a mixture of the compound obtained by the above reaction and the unreacted surfactant and / or the unreacted divalent fatty acid or polyvalent fatty acid, amino acid, targeting protein, targeting polypeptide, and / or targeting polysaccharide.
[0107] According to the composite body described in any one of Technical Solutions 1 to 29, the surfactant is one or more selected from fatty alcohol polyoxyethylene ether, fatty acid polyoxyethylene ester, alkyl polyglucoside, sucrose fatty acid ester, sorbitan fatty acid ester, polyoxyethylene sorbitan fatty acid ester, mannosylerythritol lipid, and N-fatty acyl-N-methylglucosamine.
[0108] According to the composite body described in any one of Technical Solutions 1 to 30, the microbial infection includes an infection caused by any one or more of virus, bacterium, fungus, chlamydia or mycoplasma.
[0109] A preparation for preventing, inhibiting or treating microbial infection prepared by using the composite body described in any one of Technical Solutions 1 to 31.
[0110] According to the preparation described in Technical Solution 32, the preparation is a pharmaceutical preparation or an environmental disinfection and sterilization preparation.
[0111] According to the preparation described in Technical Solution 33, the pharmaceutical preparation is one selected from inhalants, nasal sprays, injections, oral preparations, and topical skin dosage forms.
[0112] Use of the composite body described in any one of Technical Solutions 1 to 31 in the preparation of a pharmaceutical preparation or an environmental disinfection and sterilization microbial reagent for preventing, inhibiting and / or treating microbial infection.
[0113] According to the use described in Technical Solution 35, the microbe is any one or more selected from virus, bacterium, fungus, chlamydia or mycoplasma.
[0114] According to the use described in Technical Solution 36, the virus is an enveloped virus and / or a non-enveloped virus.
[0115] According to the use described in Technical Solution 37, the enveloped virus is one or more of coronavirus, influenza virus, human immunodeficiency virus, hepatitis B virus, hepatitis C virus, herpes virus, Zika virus, dengue virus, Japanese encephalitis virus, Ebola virus, rabies virus, and hantavirus, and the non-enveloped virus is one or more of hepatitis A virus, human papillomavirus, poliovirus, and coxsackievirus.
[0116] (39) According to the use described in Technical Solution 36, the virus is any one or more of coronavirus, human immunodeficiency virus, hepatitis B virus, hepatitis C virus, herpes virus, Japanese encephalitis virus, rabies virus, human papillomavirus, and Ebola virus.
[0117] (40) According to the use described in Technical Solution 36, the bacterium is a gram-positive bacterium and / or a gram-negative bacterium, the fungus is a pathogenic fungus and / or a conditional pathogenic fungus, the chlamydia is Chlamydia trachomatis, Chlamydia pneumoniae and / or Chlamydia psittaci, and the mycoplasma includes Mycoplasma pneumoniae, Mycoplasma urealyticum, Mycoplasma hominis, and / or Mycoplasma genitalium.
[0118] (41) According to the use described in Technical Solution 36, the bacterium is one or more selected from Escherichia coli, Staphylococcus aureus, methicillin-resistant Staphylococcus aureus, Streptococcus pneumoniae, Klebsiella pneumoniae, and Pseudomonas aeruginosa, and the fungus is one or more selected from Candida albicans, Aspergillus niger, anaerobic positive bacilli, ascomycetes, Aspergillus proteus, and Microsporum canis.
[0119] (42) According to the use described in Technical Solution 36, the virus is one or more selected from H7N9 influenza virus, H5N1 influenza virus, HIV virus, novel coronavirus, HPV virus, and rabies virus.
[0120] (43) A compound having a lipophilic saturated and / or unsaturated carbon chain with a branched, cyclic structure and / or linear structure, a water-soluble molecule, a protein, polypeptide, amino acid, oligopeptide, oligosaccharide, monosaccharide and / or polysaccharide molecule that can bind to a microbial lipid membrane, microbial surface domain or cell wall, which may be added as required, and a linker molecule that may be added as required are reacted in the presence of a catalyst to obtain the complex, which is a method for preparing the complex according to any one of Technical Solutions 1 to 32.
[0121] (44) According to the method for preparing the complex described in Technical Solution 43, the complex is a product obtained by purifying the compound obtained by the reaction.
[0122] (45) A compound having a lipophilic saturated and / or unsaturated carbon chain with a branched, cyclic structure and / or linear structure, a water-soluble molecule, and at least one selected from a protein, polypeptide, amino acid, oligopeptide, oligosaccharide, monosaccharide and polysaccharide molecule that can bind to a microbial lipid membrane, virus surface domain or cell wall, which may be added as required, are physically mixed to obtain the complex, which is a method for preparing the complex according to any one of Technical Solutions 1 to 31.
[0123] (46) A substance having a carbon chain with 3 to 100 carbon atoms as an active part and at least one substance selected from a protein, polypeptide, oligopeptide, oligosaccharide, amino acid, monosaccharide, disaccharide, nucleotide, vitamin, water-soluble polymer, water-soluble polyamino acid and polysaccharide are reacted in the presence of a catalyst to obtain the complex, which is a method for preparing the complex according to any one of Technical Solutions 1 to 31, wherein the catalyst may be one or more of EDC, DCC, NHS, DMAP, HoBt and its derivative analogs, the catalyst is preferably carbodiimide and succinimide, and the molar ratio of the two is 0.1:1 to 10:1, preferably 1:1 to 1:10.
[0124] (47) According to the method for preparing the complex described in Technical Proposal 46, the complex is a product obtained by purifying a compound obtained by a reaction.
[0125] (48) A method for preparing a complex according to any one of Technical Proposals 1 to 31, wherein a substance having a carbon chain of 3 to 100 carbon atoms as an active moiety is complexed with at least one selected from proteins, polypeptides, oligopeptides, polysaccharides, oligosaccharides, amino acids, monosaccharides, disaccharides, nucleotides, vitamins, water-soluble polymers, water-soluble polyamino acids, and polysaccharide molecules by physicochemical action to obtain a complex, or directly physically mixed to obtain the complex.
[0126] Specifically, in order to solve the lack of reagents that have no toxicity or side effects in the prior art and can widely kill, prevent, or treat microbial infections, the present invention provides the following Third Technical Proposal.
[0127] (1) A complex capable of preventing, inhibiting, and / or treating viral or bacterial infections, comprising an active moiety, a binding moiety, and a water-soluble moiety, wherein the virus is one or more viruses selected from novel coronavirus, influenza virus, human immunodeficiency virus, hepatitis B virus, human herpes virus, Ebola virus, rabies virus, and human papillomavirus, and the bacterium is one or more bacteria selected from Escherichia coli, Staphylococcus aureus, methicillin-resistant Staphylococcus aureus, Streptococcus pneumoniae, Klebsiella pneumoniae, and Pseudomonas aeruginosa, the active moiety is a lipophilic saturated and / or unsaturated carbon chain having a branched, cyclic structure, and / or a linear structure, the carbon chain is a molecule or a residue of a molecule, the carbon chain is a carbon chain having 3 to 100 carbon atoms, and here, the active moiety is a carbon chain having 3 to 100 carbon atoms or a residue of a carbon chain formed by saturated and / or unsaturated fatty acids, The water-soluble portion is a molecule or a residue of a molecule that is soluble in water, and the molecule contains one or more functional groups selected from an amide group, a phosphoryloxy group, a carboxylic acid group, a phosphoric acid group, a sulfonic acid group, a sulfonyloxy group, a hydroxy group, a quaternary ammonium group, a thioether group, a disulfide bond, an ether group, a mercapto group, an aldehyde group, an ester group, an amine group, an amino group, a urea group, and a guanidino group. The water-soluble portion may be the above one or more functional groups linked to a carbon chain that is the active portion. The binding portion is a molecule or a residue of a molecule that can bind to a microbial lipid membrane, a microbial surface protein, a microbial surface polysaccharide, or a cell wall component, or can bind to a polysaccharide, a protein, or a polypeptide in a microorganism. The binding portion is the same as the water-soluble portion, that is, it may be a protein, a polypeptide, an amino acid, an oligopeptide, an oligosaccharide, a monosaccharide, and / or a polysaccharide molecule or a residue thereof that can bind to a microbial lipid membrane or a surface domain. Here, the number of any one of the active portion, the water-soluble portion, and the binding portion may be one or more.
[0128] (2) According to the complex described in Technical Proposal 1, the number of carbon atoms is 3 to 48.
[0129] (3) According to the complex described in Technical Proposal 1, the number of carbon atoms is 3 to 26.
[0130] (4) According to the complex described in Technical Proposal 1, the water-soluble portion is a water-soluble molecule or a residue of a molecule containing one or more groups selected from a mercapto group, an amino group, a phosphoric acid group, a carboxylic acid group, a sulfonic acid group, a hydroxy group, an amine group, a urea group, a guanidino group, and a disulfide group. The binding moiety has a group that exerts a binding action, that is, it can bind to a microbial lipid membrane, a microbial surface protein, a microbial surface polysaccharide, or a cell wall component, or can bind to a polysaccharide, protein, or polypeptide in a microorganism. This group is derived from a water-soluble moiety or is derived from two or more groups selected from a mercapto group, an amino group, a phosphate group, a carboxylic acid group, a sulfonic acid group, a hydroxy group, an amine group, a urea group, a guanidino group, and a disulfide group that independently serve as a binding moiety, or is derived from one or two or more groups selected from a mercapto group, an amino group, a phosphate group, a carboxylic acid group, a sulfonic acid group, a hydroxy group, an amine group, a urea group, a guanidino group, and a disulfide group that provide a linkage between carbon chains. Thereby, the complex has one or two or more groups among a mercapto group, an amino group, a phosphate group, a carboxylic acid group, a sulfonic acid group, a hydroxy group, an amine group, a urea group, a guanidino group, and a disulfide group.
[0131] (5) According to the complex described in Technical Proposal 4, the binding moiety is one or two or more selected from a divalent fatty acid or a polyvalent fatty acid, an amino acid, a targeting protein, a targeting polypeptide, and a targeting polysaccharide.
[0132] (6) According to the complex described in Technical Proposal 4, the complex is a complex formed by linking a fatty acid having 3 to 50 carbon atoms and a water-soluble amino acid, or the complex is a complex formed by linking a fatty acid having 3 to 50 carbon atoms to a targeting polypeptide, or the complex is a complex formed by reacting a fatty acid having 3 to 50 carbon atoms, a targeting polypeptide, and PEG, or the complex is a complex formed by reacting a surfactant with one or two or more selected from a divalent fatty acid or a polyvalent fatty acid, an amino acid, a targeting protein, a targeting polypeptide, and a targeting polysaccharide.
[0133] According to the complex described in Technical Solution 4, the saturated and / or unsaturated fatty acid is selected from saturated or unsaturated fatty acids having 3 to 50 carbon atoms, and the fatty acid contains a double bond, a triple bond, a hydroxy group, an amino group, and / or is a fatty acid or amino acid substituted with oxygen, and is a monobasic acid, a dibasic acid or a polybasic acid.
[0134] According to the complex described in Technical Solution 4, the saturated and / or unsaturated fatty acid is a saturated fatty acid having 3 to 46 carbon atoms, a monoenoic acid having 3 to 34 carbon atoms, a dienoic acid having 5 to 30 carbon atoms, a trienoic acid having 7 to 30 carbon atoms, a tetraenoic acid having 12 to 38 carbon atoms, a pentaenoic acid having 12 to 38 carbon atoms, a hexaenoic acid having 22 to 38 carbon atoms, an acetylene acid having 6 to 22 carbon atoms, a diacetylene acid having 10 to 22 carbon atoms, a triacetylene acid having 12 to 22 carbon atoms, an eninic acid having 8 to 20 carbon atoms, a fatty acid having a main chain carbon number of 3 to 30 and a branched carbon number of 1 to 10 and / or a hydroxy group of 1 to 3, a saturated linear and branched dicarboxylic acid and tricarboxylic acid having 3 to 38 carbon atoms, an unsaturated linear or branched dicarboxylic acid and tricarboxylic acid having 4 to 18 carbon atoms which may be substituted with a hydroxy group, a carboxylic acid substituted with an amino group, a hydroxy group, an oxo group and / or a methyl group having 3 to 18 carbon atoms, an N-fatty acyl amino acid having 6 to 30 carbon atoms, an amino acid containing two or more fatty acyls, and a polycarboxylic acid linked by a thioether bond and an amide bond, and is one or more selected from these.
[0135] According to the complex described in Technical Solution 4, the saturated and / or unsaturated fatty acid is one or more selected from fumaric acid, caprylic acid, glutaconic acid, hexanoic acid, nonanoic acid, dodecanoic acid, tetradecanoic acid, hexadecanoic acid, octadecanoic acid, eicosanoic acid, oleic acid, linoleic acid, linolenic acid, eicosapentaenoic acid, docosapentaenoic acid, docosahexaenoic acid, pentacosanoic acid, enanthic acid, decanoic acid, dodecenoic acid, tetradecenoic acid, dotriacontanehexaenoic acid, octacosanoic acid, or a carbon chain residue formed by these.
[0136] According to the complex described in Technical Solution 4, the water-soluble portion is a molecule or a residue of a molecule containing one or more groups selected from a mercapto group, an amino group, a carboxylic acid group, a hydroxy group, and a disulfide group, and the molecule is one or more water-soluble macromolecules or residues thereof selected from proteins, polysaccharides, nucleic acids, and artificially synthesized water-soluble polymers. and / or one or more medium molecules or residues thereof selected from polypeptides, oligopeptides, oligosaccharides, oligonucleotides, and artificially synthesized medium molecular weight water-soluble polymers. and / or one or more water-soluble small molecules or residues thereof selected from amino acids, monosaccharides, disaccharides, nucleotides, water-soluble vitamins, and deoxyribonucleotides. and / or a molecule or a residue of a molecule linked to the carbon chain that is the active portion, and the molecule or the residue of the molecule contains one or more groups selected from a mercapto group, an amino group, a carboxylic acid group, a hydroxy group, and a disulfide group.
[0137] (11) According to the complex described in Technical Solution 10, the protein that is the water-soluble macromolecule is one or more water-soluble macromolecules selected from serum albumin, immunoglobulins, water-soluble collagen, chaperones, water-soluble glycoproteins, and CD14, and the polysaccharide that is the macromolecule is one or more water-soluble macromolecules selected from glucan, hyaluronic acid, sialic acid, heparan sulfate, heparin sulfate, chondroitin sulfate, dermatan sulfate, keratan sulfate, acetylated water-soluble cellulose derivatives, β-cyclodextrin and its derivatives, and water-soluble chitosan derivatives, and the water-soluble polymer that is the macromolecule is one or more water-soluble macromolecules selected from polyethylene glycol and carboxylated or aminated polyethylene glycol, polyvinyl alcohol and carboxylated or quaternized polyvinyl alcohol, polyacrylic acid and ammonium polyacrylate. The medium molecular weight water-soluble polymer is one or more substances selected from a targeting polypeptide, an oligopeptide, an oligosaccharide, an oligonucleotide, and / or a water-soluble polyamino acid. The water-soluble small molecule monosaccharide and / or disaccharide is one or more selected from glucose, fructose, rhamnose, sorbose, sucrose, maltose, lactose, and trehalose. The water-soluble small molecule nucleotide and / or deoxyribonucleotide is selected from adenylate, guanylate, uridylate, cytidylate, thymidylate, inosine, deoxyadenylate, deoxyguanylate, deoxycytidylate, and deoxythymidylate. The water-soluble small molecule amino acid is one or more selected from serine, threonine, cysteine, asparagine, glutamine, tyrosine, lysine, arginine, histidine, aspartic acid, glutamic acid, citrulline, ornithine, taurine, and aminobutyric acid. The water-soluble small molecule vitamin is one or more selected from vitamin B1, pantothenic acid, vitamin B6, and vitamin C.
[0138] (12) According to the complex described in Technical Solution 11, the targeting polypeptide includes any one of a specific targeting microbial lipid membrane, the cell walls of bacteria and fungi, the protein of the viral surface protein domain, or a neutralizing antibody fragment.
[0139] (13) According to the complex described in Technical Solution 11, the water-soluble polyamino acid is selected from polyglutamic acid, polylysine, and / or polyaspartic acid.
[0140] (14) According to the complex described in Technical Solution 1, the binding part is the same as the water-soluble part, that is, a microbial lipid membrane, a protein, polypeptide, oligopeptide, oligosaccharide, monosaccharide, disaccharide, amino acid, nucleotide, vitamin, water-soluble polymer, water-soluble polyamino acid and / or polysaccharide molecule that can bind to the surface domain, and the molecule or the residue of the molecule contains one or more groups selected from a mercapto group, an amino group, a carboxylic acid group, a hydroxy group, and a disulfide group.
[0141] (15) According to the complex described in Technical Solution 1, it is a compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms with a protein, polypeptide, oligopeptide, oligosaccharide, monosaccharide, disaccharide, nucleotide, vitamin, amino acid, water-soluble polymer, water-soluble polyamino acid and / or polysaccharide, or a compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 50 carbon atoms with a protein, polypeptide, oligopeptide, oligosaccharide, monosaccharide, disaccharide, nucleotide, vitamin, amino acid, water-soluble polymer, water-soluble polyamino acid and / or polysaccharide molecule, and a mixture of the unreacted fatty acid and / or the unreacted protein, polypeptide, oligopeptide, oligosaccharide, monosaccharide, disaccharide, nucleotide, vitamin, amino acid, water-soluble polymer, water-soluble polyamino acid and / or polysaccharide molecule.
[0142] (16) According to the complex described in Technical Solution 1, it is a complex obtained by complexing a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms with a protein, polypeptide, oligopeptide, oligosaccharide, monosaccharide, disaccharide, nucleotide, vitamin, amino acid, water-soluble polymer, water-soluble polyamino acid and / or polysaccharide molecule by physicochemical action, or a mixture directly physically mixed, and the physicochemical action includes a hydrogen bond or a van der Waals force or a combination of both of these actions.
[0143] According to the complex described in Technical Proposal 15, it is a compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms with at least one selected from proteins, polypeptides, oligopeptides, and amino acids, or a compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms with at least one selected from proteins, polypeptides, oligopeptides, and amino acids, and a mixture of unreacted fatty acid and / or at least one selected from unreacted proteins, polypeptides, oligopeptides, and amino acids.
[0144] (18) According to the complex described in Technical Proposal 15, it is a compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms, PEG, and at least one selected from proteins, polypeptides, oligopeptides, and amino acids, or a compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms, PEG, and at least one selected from proteins, polypeptides, oligopeptides, and amino acids, and a mixture of unreacted fatty acid, unreacted PEG, and / or at least one selected from unreacted proteins, polypeptides, oligopeptides, and amino acids.
[0145] (19) According to the complex described in Technical Proposal 15, it is a compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms with a polysaccharide, monosaccharide, disaccharide, and / or oligosaccharide, or a compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms with a polysaccharide, monosaccharide, disaccharide, and / or oligosaccharide, and a mixture of unreacted fatty acid and / or unreacted polysaccharide, monosaccharide, disaccharide, and / or oligosaccharide.
[0146] According to the complex described in Technical Solution 15, it is a compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms, PEG, and at least one selected from polysaccharides, monosaccharides, disaccharides, and oligosaccharides, or a mixture of a compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms, PEG, and at least one selected from polysaccharides, monosaccharides, disaccharides, and oligosaccharides with unreacted fatty acid, unreacted PEG, and / or unreacted polysaccharide, monosaccharide, disaccharide, and / or oligosaccharide.
[0147] (21) According to the complex described in Technical Solution 15, the protein is one or more selected from serum albumin, immunoglobulin, water-soluble collagen, chaperone, water-soluble glycoprotein, and CD14.
[0148] (22) According to the complex described in Technical Solution 15, the polysaccharide is one or more selected from glucan and / or hyaluronic acid, sialic acid, heparin sulfate, heparan sulfate, chondroitin sulfate, dermatan sulfate, keratan sulfate, acetylated water-soluble cellulose derivative, β-cyclodextrin and its derivatives, and water-soluble chitosan derivative.
[0149] (23) According to the complex described in Technical Solution 15, it is a compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms, a linker, and a protein containing a mercapto group, or a mixture of the compound obtained by the above reaction, unreacted fatty acid, unreacted linker, and / or unreacted protein containing a mercapto group, where the linker is one or more of amino acid, succinic acid, butadienoic acid, glutaconic acid, hexaminedioic acid, urethane, short peptide, N-hydroxybutenimide, polyethylene glycol, and derivatives of the above compounds.
[0150] According to the composite described in Technical Proposal 23, the composite is a compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms, N-hydroxybutenimide, and a protein containing a mercapto group, or a mixture of a compound obtained by the above reaction, an unreacted fatty acid, an unreacted N-hydroxybutenimide, and / or a protein containing an unreacted mercapto group.
[0151] (25) According to the composite described in Technical Proposal 15, it is a compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms, cystamine, and at least one selected from polysaccharides, monosaccharides, disaccharides, and oligosaccharides, or a compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 50 carbon atoms, cystamine, and at least one selected from polysaccharides, monosaccharides, disaccharides, and oligosaccharides, and a mixture of the unreacted fatty acid, at least one selected from the unreacted polysaccharides, monosaccharides, disaccharides, and oligosaccharides, and / or unreacted cystamine.
[0152] (26) According to the composite described in any one of Technical Proposals 15 to 25, the compound obtained by the reaction contains one or more of an amide group, an ester group, a thioether group, or an ether group, and these groups function as a part for linking a water-soluble part and an active part.
[0153] (27) According to the composite described in any one of Technical Proposals 4 to 25, the saturated and / or unsaturated fatty acid has 3 to 50 carbon atoms.
[0154] (28) According to the composite described in Technical Proposal 27, the number of carbon atoms is 3 to 48.
[0155] (29) According to the composite described in Technical Proposal 27, the number of carbon atoms is 3 to 26.
[0156] According to the complex according to any one of Technical Solutions 4 to 25, the saturated and / or unsaturated fatty acid is a fatty acid having 3 to 40 carbon atoms containing 1 to 8 C=C double bonds, a fatty acid containing 1 to 7 C=C double bonds, a fatty acid containing 1 to 6 double bonds, a fatty acid containing 1 to 5 double bonds, a fatty acid containing 1 to 4 double bonds, a fatty acid containing 1 to 3 double bonds, or a fatty acid containing 1 to 2 double bonds.
[0157] (31) According to the complex according to any one of Technical Solutions 4 to 25, the saturated and / or unsaturated fatty acid is a fatty acid having 3 to 30 carbon atoms containing 1 to 6 double bonds.
[0158] (32) According to the complex according to any one of Technical Solutions 4 to 25, the saturated and / or unsaturated fatty acid has 3 to 30 carbon atoms.
[0159] (33) According to the complex according to any one of Technical Solutions 4 to 25, the saturated and / or unsaturated fatty acid is one or more fatty acids selected from fumaric acid, caprylic acid, glutaconic acid, hexanoic acid, nonanoic acid, dodecanoic acid, tetradecanoic acid, hexadecanoic acid, octadecanoic acid, eicosanoic acid, oleic acid, linoleic acid, linolenic acid, eicosapentaenoic acid, docosapentaenoic acid, docosahexaenoic acid, pentacosanic acid, enanthic acid, decanoic acid, dodecenoic acid, tetradecenoic acid, dotriacontanehexaenoic acid, and octacosanoic acid.
[0160] (34) According to the complex according to any one of Technical Solutions 4 to 25, the protein is human serum protein, or bovine serum protein, or CD14, or the polysaccharide is glucan and / or hyaluronic acid.
[0161] (35) The present invention further provides a preparation for preventing, inhibiting or treating microbial infection prepared from the above-described complex.
[0162] According to the preparation described in the present invention, the preparation is a pharmaceutical preparation or an environmental disinfection and sterilization preparation.
[0163] According to the preparation described in the present invention, the pharmaceutical preparation is one selected from the group consisting of an inhalant, a nasal spray, an injection, an oral preparation, and a topical skin dosage form.
[0164] Use of the complex described in the present invention in the preparation of a pharmaceutical preparation or an environmental disinfection and sterilization microbial reagent for preventing, inhibiting and / or treating microbial infections.
[0165] According to the use described in the present invention, the microorganism is any one or two selected from the group consisting of viruses and bacteria.
[0166] According to the use described in the present invention, the virus is an enveloped virus and / or a non-enveloped virus.
[0167] According to the use described in the present invention, the virus is one or more viruses selected from the group consisting of novel coronavirus, influenza virus, human immunodeficiency virus (HIV), hepatitis B virus, human herpes virus, Ebola virus, rabies virus, and human papillomavirus (HPV), and the bacterium is one or more bacteria selected from the group consisting of Escherichia coli, Staphylococcus aureus, methicillin-resistant Staphylococcus aureus, Streptococcus pneumoniae, Klebsiella pneumoniae, and Pseudomonas aeruginosa.
[0168] According to the use described in the present invention, the virus is one or more selected from the group consisting of H7N9 influenza virus, H5N1 influenza virus, HIV virus, novel coronavirus, HPV virus, and rabies virus.
[0169] ( 39 )The present invention further provides a method for preparing the complex, which comprises reacting a fatty acid having a branched, cyclic structure and / or a linear structure with a lipophilic saturated and / or unsaturated carbon chain, a water-soluble molecule, and optionally a protein, polypeptide, amino acid, oligopeptide, oligosaccharide, monosaccharide and / or polysaccharide molecule that can bind to a microbial lipid membrane, a microbial surface domain or a cell wall, and an optionally added linker molecule in the presence of a catalyst to obtain the complex.
[0170] More preferably, according to the method for preparing the complex described in the present invention, the complex is a product obtained by purifying the compound obtained by the reaction.
[0171] ( 40 ) The present invention further provides a method for preparing the complex, which comprises physically mixing a fatty acid having a branched, cyclic structure and / or a linear structure with a lipophilic saturated and / or unsaturated carbon chain, a water-soluble molecule, and optionally a protein, polypeptide, amino acid, oligopeptide, oligosaccharide, monosaccharide and / or polysaccharide molecule that can bind to a microbial lipid membrane, a virus surface domain or a cell wall to obtain the complex.
[0172] ( 41 ) The present invention further provides a method for preparing the complex, which comprises reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms with any one substance selected from proteins, polypeptides, oligopeptides, polysaccharides, oligosaccharides, monosaccharides, disaccharides, nucleotides, vitamins, amino acids, water-soluble polymers, water-soluble polyamino acids and / or polysaccharides in the presence of a catalyst to obtain the complex.
[0173] More preferably, the complex is a product obtained by purifying the compound obtained by the reaction.
[0174] ( 42 )The present invention further provides a method for preparing the complex, which comprises complexing a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms with a protein, polypeptide, oligopeptide, polysaccharide, oligosaccharide, monosaccharide, disaccharide, nucleotide, vitamin, amino acid, water-soluble polymer, water-soluble polyamino acid and / or polysaccharide molecule by physicochemical action to obtain the complex, or directly physically mixing them to obtain the complex.
[0175] Use of the complex and its preparation of the present invention, which have the effect of preventing and treating viral, bacterial and fungal infections, in the prevention or treatment of various viral, bacterial and fungal infectious diseases. The specific usage methods are as follows: Using it before infection to prevent viral, bacterial and fungal infections. Using it after infection to kill viruses, bacteria and fungi in the body, and Including killing and disposing of the article environment to prevent the transmission of viruses, bacteria and fungi.
[0176] Compared with the prior art, the present invention has the following beneficial effects. (1) The effect of the complex provided by the present invention on viruses is not affected by virus mutation. The action target of the complex provided by the present invention is the basic structure of the virus - envelope and nucleocapsid. In the case of enveloped viruses, the complex destroys the virus envelope so that the virus loses its ability to invade cells. In the case of non-enveloped viruses, the complex directly wraps the virus nucleocapsid for hydrophobic isolation so that the virus cannot invade cells. The complex does not cause dysfunction due to virus mutation. (2) The complex provided by the present invention can kill drug-resistant microorganisms and does not cause drug resistance in microorganisms. Bacteria show resistance because they have resistance genes in their bodies, which express enzymes that break down antibiotics and nullify the effects of antibiotics. The mechanism by which the complex of the present invention kills microorganisms is different from that of antibiotics. It acts directly on the basic structure of microorganisms - the lipid membrane. By dissolving the acting part into the lipid membrane, it affects the stable state of the lipid membrane and achieves a killing effect by destroying the cell wall and cell membrane. Therefore, it is not affected by the enzymes that break down antibiotics in resistant bacteria. (3) The complex provided by the present invention is safe for human cells. Virus particles and the cells of bacteria and fungi are much smaller than human cells. The therapeutic dose of the complex preferentially binds to and acts on viruses, bacteria, and fungi. Cell experiments have verified that at the therapeutic dose, the complex does not significantly affect the cell membrane. The complex is safe for human cells. 。 (4) The complex provided by the present invention can function in different regions according to the molecular size. The large - molecule complex can stay on the mucosal surface of the respiratory tract or in the blood circulation, inactivate viruses, bacteria, or fungi most quickly, and prevent the spread of viruses, bacteria, or fungi in the body. The large - molecule complex cannot enter normal tissues and can only enter the inflammatory sites after virus, bacteria, or fungal infection. However, the small - molecule complex can enter the tissue spaces and interstitial fluid through the blood vessel wall and target and kill viruses, bacteria, or fungi. (5) Fatty acids, aliphatic alcohols, fat - soluble vitamins, and steroids are insoluble in water or have extremely low water solubility and cannot be directly injected into the body. Direct intravenous injection will cause pulmonary embolism. The absorption of fatty acids in food is absorbed by the human body in the form of an emulsion, passes through the lymphatic system, through lymphatic vessels and the thoracic duct, and returns to the blood circulation in the form of chylomicrons. Furthermore, fatty acids are encapsulated in the emulsion in a form that non - covalently binds to proteins. The hydrophobic groups in this form are encapsulated inside and do not come into contact with infected viruses or bacteria, and thus do not exert a bactericidal and antiviral effect. By converting fat - soluble hydrophobic compounds into aqueous - solution compounds with high affinity for pathogenic microorganisms, the above problems can be avoided.
[0177] Furthermore, after deeply studying the working mechanism of the present invention, the present invention discovers and provides the following fourth technical solution.
[0178] 1. A water-soluble carbon chain substance that regulates the transmembrane transport and / or fluidity of cell membranes, comprising an active portion, a binding portion, and a water-soluble portion, wherein the active portion is a lipophilic saturated and / or unsaturated carbon chain having a branched, cyclic structure and / or a linear structure, the carbon chain is a molecule or a residue of a molecule, the carbon chain is a carbon chain having 3 to 100 carbon atoms, and wherein the active portion is a carbon chain having 3 to 100 carbon atoms or a residue of a carbon chain formed by any one or more of saturated and / or unsaturated fatty acids, aliphatic hydrocarbons or cyclic hydrocarbons, or aromatic compounds or heterocyclic compounds, or salts, alcohols, ethers, esters or other derivatives thereof, the water-soluble portion is a molecule or a residue of a molecule that is soluble in water, the molecule contains one or more functional groups selected from an amide group, a phosphoryloxy group, a carboxylic acid group, a phosphate group, a sulfonic acid group, a sulfonyloxy group, a hydroxy group, a quaternary ammonium group, a thioether group, a disulfide bond, an ether group, a mercapto group, an aldehyde group, an ester group, an amine group, an amino group, a urea group, a guanidino group, and the water-soluble portion may be one or more of the above functional groups linked to the carbon chain that is the active portion, the binding portion is a molecule or a residue of a molecule that can bind to a microbial lipid membrane, a microbial surface protein, a microbial surface polysaccharide or a cell wall component, or can bind to a polysaccharide or a protein or a polypeptide in the body of a microorganism, a plant, an animal or a human, or a molecule or a residue of a molecule that can bind to a cell membrane or a surface polysaccharide or a cell wall component of a cell membrane of a plant, an animal or a human tissue, and the binding portion is the same as the water-soluble portion, that is, it may be a protein, a polypeptide, an amino acid, an oligopeptide, an oligosaccharide, a monosaccharide, a disaccharide, an amino acid, a nucleotide, a vitamin, a water-soluble polymer, a water-soluble polyamino acid and / or a polysaccharide molecule or a residue thereof that can bind to a microbial lipid membrane or to a surface domain of a cell membrane of a plant, an animal or a human tissue, Here, the number of any one of the action part, the water-soluble part, and the binding part may be one or two or more.
[0179] 2. According to the water-soluble carbon chain substance described in Technical Proposal 1, the number of carbon atoms is 3 to 50, preferably 3 to 48, more preferably 3 to 26.
[0180] 3. According to the water-soluble carbon chain substance described in Technical Proposal 1, the water-soluble part is a water-soluble molecule or a residue of a molecule containing one or more groups selected from a mercapto group, an amino group, a phosphate group, a carboxylic acid group, a sulfonic acid group, a hydroxy group, an amine group, a urea group, a guanidino group, and a disulfide group. The binding part has a group that exerts a binding action, that is, it can bind to a microbial lipid membrane, a microbial surface protein, a microbial surface polysaccharide, or a cell wall component, or can bind to a polysaccharide, protein, or polypeptide in the body of a microorganism, a plant, an animal, or a human, or can bind to a cell membrane, a surface polysaccharide of a cell membrane, or a cell wall component of a tissue of a plant, an animal, or a human. This group is derived from the water-soluble part, or is derived from one or more groups selected from a mercapto group, an amino group, a phosphate group, a carboxylic acid group, a sulfonic acid group, a hydroxy group, an amine group, a urea group, a guanidino group, and a disulfide group that independently serve as the binding part, or is derived from one or more groups selected from a mercapto group, an amino group, a phosphate group, a carboxylic acid group, a sulfonic acid group, a hydroxy group, an amine group, a urea group, a guanidino group, and a disulfide group that provide a linkage between carbon chains. As a result, the complex has one or more groups selected from a mercapto group, an amino group, a phosphate group, a carboxylic acid group, a sulfonic acid group, a hydroxy group, an amine group, a urea group, a guanidino group, and a disulfide group.
[0181] 4. According to the water-soluble carbon chain substance described in any one of Technical Proposals 1 to 3, the binding part is one or more selected from a divalent fatty acid or a polyvalent fatty acid, an amino acid, a targeting protein, a targeting polypeptide, and a targeting polysaccharide.
[0182] According to the water-soluble carbon chain substance described in any one of Technical Solutions 1 to 3, the water-soluble carbon chain substance is a compound, a complex or a mixture.
[0183] According to the water-soluble carbon chain substance described in Technical Solution 5, the water-soluble carbon chain substance is a complex formed by linking a fatty acid having 3 to 50 carbon atoms and a water-soluble amino acid, a complex formed by linking a fatty acid having 3 to 50 carbon atoms to a targeting polypeptide, a complex formed by reacting a fatty acid having 3 to 50 carbon atoms, a targeting polypeptide and PEG, or a complex formed by reacting a surfactant with one or more selected from dibasic fatty acids or polybasic fatty acids, amino acids, targeting proteins, targeting polypeptides, and targeting polysaccharides.
[0184] According to the water-soluble carbon chain substance described in any one of Technical Solutions 1 to 4, the saturated and / or unsaturated fatty acid is selected from saturated fatty acids or unsaturated fatty acids having 3 to 50 carbon atoms, and the fatty acid contains a double bond, a triple bond, a hydroxy group, an amino group, and / or is a fatty acid or an amino acid substituted with oxygen, and is a monobasic acid, a dibasic acid or a polybasic acid.
[0185] 8. According to the water-soluble carbon chain substance described in Technical Solution 7, the saturated and / or unsaturated fatty acids are saturated fatty acids having 3 to 46 carbon atoms, monoenoic acids having 3 to 34 carbon atoms, dienoic acids having 5 to 30 carbon atoms, trienoic acids having 7 to 30 carbon atoms, tetraenoic acids having 12 to 38 carbon atoms, pentaenoic acids having 12 to 38 carbon atoms, hexaenoic acids having 22 to 38 carbon atoms, acetylenic acids having 6 to 22 carbon atoms, diacetylenic acids having 10 to 22 carbon atoms, triacetylenic acids having 12 to 22 carbon atoms, eninic acids having 8 to 20 carbon atoms, fatty acids having a main chain carbon number of 3 to 30 and a branched carbon number of 1 to 10 and / or 1 to 3 hydroxy groups, saturated linear and branched dicarboxylic acids and tricarboxylic acids having 3 to 38 carbon atoms, unsaturated linear or branched dicarboxylic acids and tricarboxylic acids having 4 to 18 carbon atoms which may be substituted with a hydroxy group, carboxylic acids substituted with an amino group, a hydroxy group, an oxo group and / or a methyl group having 3 to 18 carbon atoms, N-fatty acyl amino acids having 6 to 30 carbon atoms, amino acids containing two or more fatty acyls, and polycarboxylic acids linked by thioether bonds and amide bonds, and are one or more selected from the group consisting of these.
[0186] 9. According to the water-soluble carbon chain substance described in Technical Solution 7, the saturated and / or unsaturated fatty acids are one or more selected from the group consisting of fumaric acid, caprylic acid, octenoic acid, glutaconic acid, hexanoic acid, suberic acid, nonanoic acid, dodecanoic acid, dodecanedioic acid, tridecanoic acid, tridecanedioic acid, tetradecanoic acid, hexadecanoic acid, hexadecanedioic acid, octadecanoic acid, eicosanoic acid, eicosanedioic acid, oleic acid, linoleic acid, linolenic acid, eicosapentaenoic acid, cetoleic acid, docosapentaenoic acid, docosahexaenoic acid, pentacosanoic acid, enanthic acid, decanoic acid, undecylenic acid, dodecenoic acid, tetradecenoic acid, hexadecenoic acid, triacontenoic acid, dotriacontanehexaenoic acid, octacosanoic acid, or carbon chain residues formed by these.
[0187] 10. According to the water-soluble carbon chain substance described in any one of Technical Solutions 1 to 4, the water-soluble part is a molecule or a residue of a molecule containing one or more groups selected from a mercapto group, an amino group, a carboxylic acid group, a hydroxy group, and a disulfide group, and the molecule is one or more water-soluble macromolecules or residues thereof selected from proteins, polysaccharides, nucleic acids, and artificially synthesized water-soluble polymers, and / or one or more medium molecules or residues thereof selected from polypeptides, oligopeptides, oligosaccharides, oligonucleotides, and artificially synthesized medium molecular weight water-soluble polymers, and / or one or more water-soluble small molecules or residues thereof selected from amino acids, monosaccharides, disaccharides, nucleotides, water-soluble vitamins, and deoxyribonucleotides, and / or a molecule or a residue of a molecule linked to the carbon chain which is the active part, and the molecule or the residue of the molecule contains one or more groups selected from a mercapto group, an amino group, a carboxylic acid group, a hydroxy group, and a disulfide group.
[0188] 11. According to the water-soluble carbon chain substance described in Technical Solution 10, the protein which is the water-soluble macromolecule is one or more water-soluble macromolecules selected from serum albumin, immunoglobulin, water-soluble collagen, chaperone, water-soluble glycoprotein, and CD14, the polysaccharide which is the macromolecule is one or more water-soluble macromolecules selected from glucan, hyaluronic acid, sialic acid, heparan sulfate, heparin sulfate, chondroitin sulfate, dermatan sulfate, keratan sulfate, acetylated water-soluble cellulose derivative, β-cyclodextrin and its derivatives, and water-soluble chitosan derivatives, and the water-soluble polymer which is the macromolecule is one or more water-soluble macromolecules selected from polyethylene glycol and carboxylated or aminated polyethylene glycol, polyvinyl alcohol and carboxylated or quaternized polyvinyl alcohol, polyacrylic acid, and ammonium polyacrylate, The medium molecular weight water-soluble polymer is one or more substances selected from targeting polypeptides, oligopeptides, oligosaccharides, oligonucleotides and / or water-soluble polyamino acids, The water-soluble small molecule monosaccharides and / or disaccharides are one or more selected from glucose, fructose, rhamnose, sorbose, sucrose, maltose, lactose, and trehalose. The water-soluble small molecule nucleotides and / or deoxyribonucleotides are selected from adenylate, guanylate, uridylate, cytidylate, thymidylate, inosine, deoxyadenylate, deoxyguanylate, deoxycytidylate, deoxythymidylate. The water-soluble small molecule amino acids are one or more selected from serine, threonine, cysteine, asparagine, glutamine, tyrosine, lysine, arginine, histidine, aspartic acid, glutamic acid, citrulline, ornithine, taurine, and aminobutyric acid. The water-soluble small molecule vitamins are one or more selected from vitamin B1, pantothenic acid, vitamin B6, and vitamin C.
[0189] 12. According to the water-soluble carbon chain substance described in Technical Solution 11, the targeting polypeptide includes any one of specific targeting microbial lipid membranes, bacterial and fungal cell walls, proteins of viral surface protein domains, or neutralizing antibody fragments.
[0190] 13. According to the water-soluble carbon chain substance described in Technical Solution 11, the water-soluble polyamino acid is selected from polyglutamic acid, polylysine and / or polyaspartic acid.
[0191] 14. According to the water-soluble carbon chain substance described in Technical Proposal 1, the binding moiety is the same as the water-soluble moiety, that is, a protein, polypeptide, oligopeptide, oligosaccharide, monosaccharide, disaccharide, amino acid, nucleotide, vitamin, water-soluble polymer, water-soluble polyamino acid and / or polysaccharide molecule or a residue of these molecules that can bind to a microbial lipid membrane, the cell membrane of an animal or human tissue, or the cell membrane surface domain, and the molecule or residue of the molecule contains one or more groups selected from a mercapto group, an amino group, a carboxylic acid group, a hydroxy group, and a disulfide group.
[0192] 15. According to the water-soluble carbon chain substance described in Technical Proposal 1, it is a compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms with at least one selected from a protein, polypeptide, oligopeptide, oligosaccharide, monosaccharide, disaccharide, nucleotide, vitamin, amino acid, water-soluble polymer, water-soluble polyamino acid, and polysaccharide molecule, or a compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms with at least one selected from a protein, polypeptide, oligopeptide, oligosaccharide, monosaccharide, disaccharide, nucleotide, vitamin, amino acid, water-soluble polymer, water-soluble polyamino acid, and polysaccharide molecule, and a mixture of the unreacted fatty acid and / or the unreacted protein, polypeptide, oligopeptide, oligosaccharide, monosaccharide, disaccharide, nucleotide, vitamin, amino acid, water-soluble polymer, water-soluble polyamino acid and / or polysaccharide molecule.
[0193] 16. According to the water-soluble carbon chain substance described in Technical Proposal 1, it is a complex obtained by complexing a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms with at least one selected from a protein, polypeptide, oligopeptide, oligosaccharide, monosaccharide, disaccharide, nucleotide, vitamin, amino acid, water-soluble polymer, water-soluble polyamino acid, and polysaccharide molecule by physicochemical action, or a mixture directly physically mixed, and the physicochemical action includes a hydrogen bond or a van der Waals force or a combination of both of these actions.
[0194] 17. According to the water-soluble carbon chain substance described in Technical Proposal 15, it is a compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms with at least one selected from proteins, polypeptides, oligopeptides, and amino acids, or a compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms with at least one selected from proteins, polypeptides, oligopeptides, and amino acids, and a mixture of unreacted fatty acids and / or at least one selected from unreacted proteins, polypeptides, oligopeptides, and amino acids.
[0195] 18. According to the water-soluble carbon chain substance described in Technical Proposal 15, it is a compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms, PEG, and at least one selected from proteins, polypeptides, oligopeptides, and amino acids, or a compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms, PEG, and at least one selected from proteins, polypeptides, oligopeptides, and amino acids, and a mixture of unreacted fatty acids, unreacted PEG, and / or at least one selected from unreacted proteins, polypeptides, oligopeptides, and amino acids.
[0196] 19. According to the complex described in Technical Proposal 15, it is a compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms with at least one selected from polysaccharides, monosaccharides, disaccharides, and oligosaccharides, or a compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms with at least one selected from polysaccharides, monosaccharides, disaccharides, and oligosaccharides, and a mixture of unreacted fatty acids and / or unreacted polysaccharides, monosaccharides, disaccharides, and / or oligosaccharides.
[0197] According to the water-soluble carbon chain substance described in Technical Proposal 15, it is a compound obtained by reacting at least one selected from saturated and / or unsaturated fatty acids having 3 to 100 carbon atoms, PEG, and polysaccharides, monosaccharides, disaccharides, and oligosaccharides, or a mixture of a compound obtained by reacting at least one selected from saturated and / or unsaturated fatty acids having 3 to 100 carbon atoms, PEG, and polysaccharides, monosaccharides, disaccharides, and oligosaccharides with unreacted fatty acids, unreacted PEG and / or unreacted polysaccharides, monosaccharides, disaccharides and / or oligosaccharides.
[0198] According to the water-soluble carbon chain substance described in Technical Proposal 15 or 16, the protein is one or more selected from serum albumin, immunoglobulin, water-soluble collagen, chaperone, water-soluble glycoprotein, and CD14.
[0199] According to the water-soluble carbon chain substance described in Technical Proposal 15 or 16, the polysaccharide is one or more selected from glucan and / or hyaluronic acid, sialic acid, heparan sulfate, heparin sulfate, chondroitin sulfate, dermatan sulfate, keratan sulfate, acetylated water-soluble cellulose derivative, β-cyclodextrin and its derivatives, and water-soluble chitosan derivative.
[0200] According to the water-soluble carbon chain substance described in Technical Proposal 15, it is a compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms, a linker, and a protein containing a mercapto group, or a mixture of the compound obtained by the above reaction, unreacted fatty acids, unreacted linkers, and / or unreacted proteins containing a mercapto group, where the linker is one or more of amino acids, succinic acid, butadienoic acid, glutaconic acid, hexamiminodiacid, urethane, short peptides, N-hydroxybutenimide, polyethylene glycol, and derivatives of the above compounds.
[0201] 24. According to the water-soluble carbon chain substance described in Technical Proposal 23, the water-soluble carbon chain substance is a compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms, N-hydroxybutenimide, and a protein containing a mercapto group, or a mixture of a compound obtained by the above reaction, an unreacted fatty acid, an unreacted N-hydroxybutenimide, and / or a protein containing an unreacted mercapto group.
[0202] 25. According to the water-soluble carbon chain substance described in Technical Proposal 15, it is a compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms, cystamine, and at least one selected from polysaccharides, monosaccharides, disaccharides, and oligosaccharides, or a compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 50 carbon atoms, cystamine, and at least one selected from polysaccharides, monosaccharides, disaccharides, and oligosaccharides, and a mixture of the unreacted fatty acid, at least one selected from the unreacted polysaccharides, monosaccharides, disaccharides, and oligosaccharides, and / or the unreacted cystamine.
[0203] 26. According to the water-soluble carbon chain substance described in any one of Technical Proposals 15 to 25, the compound obtained by the above reaction contains one or more groups among an amide group, an ester group, a thioether group, or an ether group, and these groups function as a part connecting the water-soluble part and the functional part.
[0204] 27. According to the water-soluble carbon chain substance described in any one of Technical Proposals 15 to 25, the saturated and / or unsaturated fatty acid has 3 to 50 carbon atoms, preferably 3 to 48 carbon atoms, more preferably 3 to 30 carbon atoms, and even more preferably 3 to 26 carbon atoms.
[0205] According to the water-soluble carbon chain substance described in any one of Technical Solutions 15 to 25, the saturated and / or unsaturated fatty acid is a fatty acid having 3 to 40 carbon atoms containing 1 to 8 C=C double bonds, a fatty acid containing 1 to 7 C=C double bonds, a fatty acid containing 1 to 6 double bonds, a fatty acid containing 1 to 5 double bonds, a fatty acid containing 1 to 4 double bonds, a fatty acid containing 1 to 3 double bonds, or a fatty acid containing 1 to 2 double bonds. Preferably, the saturated and / or unsaturated fatty acid is a fatty acid having 3 to 30 carbon atoms containing 1 to 6 double bonds.
[0206] According to the water-soluble carbon chain substance described in any one of Technical Solutions 15 to 25, the saturated and / or unsaturated fatty acid has 3 to 30 carbon atoms.
[0207] According to the water-soluble carbon chain substance described in any one of Technical Solutions 15 to 25, the saturated and / or unsaturated fatty acid is one or more fatty acids selected from fumaric acid, caprylic acid, octenoic acid, glutaconic acid, hexanoic acid, suberic acid, nonanoic acid, dodecanoic acid, dodecanedioic acid, tridecanoic acid, tridecanedioic acid, tetradecanoic acid, hexadecanoic acid, hexadecanedioic acid, octadecanoic acid, eicosanoic acid, eicosanedioic acid, oleic acid, linoleic acid, linolenic acid, eicosapentaenoic acid, cetoleic acid, docosapentaenoic acid, docosahexaenoic acid, pentacosanoic acid, enanthic acid, decanoic acid, undecylenic acid, dodecenoic acid, tetradecenoic acid, hexadecenoic acid, triacontenoic acid, dotriacontanehexaenoic acid, octacosanoic acid.
[0208] According to the water-soluble carbon chain substance described in any one of Technical Solutions 15 to 25, the protein is human serum protein or bovine serum protein, or CD14, or the polysaccharide is glucan and / or hyaluronic acid.
[0209] According to the water-soluble carbon chain substance described in Technical Solution 75, the saturated and / or unsaturated fatty acid has 3 to 30 carbon atoms. Preferably, the saturated and / or unsaturated fatty acid is one or more fatty acids selected from fumaric acid, caprylic acid, octenoic acid, glutaconic acid, hexanoic acid, suberic acid, nonanoic acid, dodecanoic acid, dodecanedioic acid, tridecanoic acid, tridecanedioic acid, tetradecanoic acid, hexadecanoic acid, hexadecanedioic acid, octadecanoic acid, eicosanoic acid, eicosanedioic acid, oleic acid, linoleic acid, linolenic acid, eicosapentaenoic acid, cetoleic acid, docosapentaenoic acid, docosahexaenoic acid, pentacosanic acid, enanthic acid, decanoic acid, undecylenic acid, dodecenoic acid, tetradecenoic acid, hexadecenoic acid, triacontenoic acid, dotriacontanehexaenoic acid, octacosanoic acid.
[0210] More preferably, the protein is human serum protein or bovine serum protein, or CD14, or the polysaccharide is glucan and / or hyaluronic acid.
[0211] 1. According to the water-soluble carbon chain substance described in the previous technical solution, the compound obtained by the reaction is a compound obtained by a fatty acid, albumin, or SBP1 reaction, and has one or more of the following structural formulas.
Chemical formula
Chemical formula
Chemical formula
Chemical formula
[0212] 33. According to the water-soluble carbon chain substance described in the previous technical solution, the compound obtained by the reaction is a compound obtained by reacting a monovalent fatty acid having 3 to 10 carbon atoms, PEG, and an amino acid, or a compound obtained by reacting a monovalent fatty acid having 3 to 10 carbon atoms, a saturated divalent fatty acid having 5 to 8 carbon atoms, PEG, and taurine.
[0213] 34. According to the water-soluble carbon chain substance described in the previous technical solution, the compound obtained by the reaction is a compound having at least one of the following structural formulas.
Chemical formula
[0214] According to the water-soluble carbon chain substance described in the previous technical solution, the compound obtained by the reaction is any one or more compounds having the following structural formula, which are obtained by reacting a fatty acid with a glucan.
Chemical formula
Chemical formula
Chemical formula
Chemical formula
[0215] According to the water-soluble carbon chain substance described in the previous technical solution, the compound obtained by the reaction is any one or more compounds having the following structural formula, which are obtained by reacting a fatty acid with hyaluronic acid.
Chemical formula
Chemical formula
Chemical formula
Chemical formula
[0216] According to the water-soluble carbon chain substance described in the previous technical solution, the compound obtained by the reaction is a compound obtained by reacting a fatty acid having 3 to 10 carbon atoms, PEG, and glucose.
[0217] According to the water-soluble carbon chain substance described in the previous technical solution, the compound obtained by the reaction is a compound having the following structural formula.
Chemical formula
[0218] 39. According to the water-soluble carbon chain substance described in the previous technical solution, the compound obtained by the reaction is any one or more than two compounds having a thioether bond, which are obtained by reacting a fatty acid, N-hydroxybutanimide, and a protein, and having the following structural formula.
Chemical formula
Chemical formula
Chemical formula
[0219] 40. According to the water-soluble carbon chain substance described in the previous technical solution, the compound obtained by the reaction is any one or more than two compounds having the following structural formula, which are obtained by reacting a fatty acid, cystamine, and a glucan.
Chemical formula
[0220] 41. According to the water-soluble carbon chain substance described in the previous technical solution, the compound obtained by the reaction is any one or more compounds having the following structural formula, which are obtained by reacting a fatty acid, cystamine, and hyaluronic acid.
Chemical formula
[0221] 42. According to the water-soluble carbon chain substance described in any one of the previous technical solutions, it includes a small molecule compound containing a hydroxy group and benzene rings, preferably, Flavon, Isoflavon, Anthocyanin, Soybean Isoflavon, Aloe-emodin, Grape Seed Extract, Green Tea-derived Flavon, Naringenin, Limocitrin, Baicalein, Riboflavin, Quercetin, Graphite-derived Flavon, Shinzelanin, Chrysin, Japanese Apricot Flavon, Morin, Luteolin, Mulberry Extract, Gypsum-derived Flavon, Honeysuckle-derived Flavon, Gentoflavin, Platycodon-derived Flavon, Violet-derived Flavon, Perilla-derived Flavon, Chrysanthemum-derived Flavon, Artemisinin, Red Peony-derived Flavon, Salvia-derived Flavon, Bupleurum-derived Flavon, Safflower-derived Flavon, Selaginella-derived Flavon, Jujube-derived Flavon, Lycium-derived Flavon, Rehmannia-derived Flavon, Chinese Date-derived Flavon, Schisandra-derived Flavon, Licorice-derived Flavon, Panax Notoginseng-derived Flavon, Curcumin, Apigenin, Carotene, Anthocyanidin, Lutein, Zeaxanthin, Wasabi Extract, Rutin, Scutellarein, Pollen Yellow Extract, Sage-derived Flavon, Dandelion-derived Flavon, Cinnamon-derived Flavon, Isoflavonoid, and Anthocyanidin; Rutin, Emodin, Fucoxanthin, Gallic Acid, Persimmon Peel Extract, Morin, Echinacoside, Grape Seed-derived Procyanidin, Phenolic Acid, Tea Polyphenol, Naringin, Citric Acid, Flavonol, Glycyrrhizic Acid, Cinnamic Acid, Flavonoid Glycoside, Oleic Acid, Matrine, Tanshinone, Erythrophleine, Snadigmic Acid, Perillyl Alcohol, Anisic Acid, Amrencin, Hesperidin, Granatin, Morcin, Naringin, Linarin, Gentiopicroside, Jasminosid, Naringetol, Carotene, Apigenin, Baimelin, Scutellaria Extract, King Side, Chrysanthemum Extract, Olive Extract, Oolong Tea Extract, L-Theanine, Red Wine Extract, Platycodon Glycoside, Perilla Alcohol Glycoside, Moracin, Calthamin, Pinosin, Pakiminic Acid, Caffeic Acid, Chlorogenic Acid;It contains one or more substances selected from the group consisting of resveratrol, white tea polyphenols, resveratrol disaccharide, banana-derived lutein, anthocyanidin, arachidonic acid, peanut-derived flavone, (+)-piperitol, anisofolin, flavonoid, baicalein, flavone glycoside, flavanol, red wine polyphenols, rhodiocyanin, calphenol, black tea-derived flavone, sesamin, rye wheat phenol, fucitol, seaweed polysaccharides, alginic acid, farnesin, cannabidiol, polydatin, cucurbitacin, fenugreek extract, cucurbitic acid, pollen phenol, pollen-derived flavone, pollen glycoside, pollen ester, arachidonic acid, peanut-derived flavone glycoside, peanut isoflavone, peanut isoflavone glycoside, peanut isoflavone disaccharide, peanut isoflavone trisaccharide, peanut resveratrol, peanut resveratrol disaccharide, peanut resveratrol trisaccharide, peanut resveratrol tetrasaccharide, peanut resveratrol pentasaccharide, peanut resveratrol hexasaccharide, peanut resveratrol heptasaccharide, peanut resveratrol octasaccharide, peanut resveratrol nonasaccharide, peanut resveratrol decasaccharide, peanut resveratrol undecasaccharide, catechin, epicatechin, tea polyphenols, catechol, chlorophyll, protocatechuic acid, hesperidin, anthocyanidin, anthocyanin, anthocyanin, cyanidin alcohol, glucoside, glucopyranoside, tricin, soybean isoflavone, flavanol, keltaninin, dattansoba extract, persimmon peel extract, persimmon tannic acid, punica acid, granatin, blueberry extract, resveratrol, lycopene, naringenin, morin, chlorogenic acid, chlorogenic acid triglucoside, chlorogenic acid diglucoside, chlorogenic acid methyl, chlorogenic acid ethyl, chlorogenic acid propyl, chlorogenic acid butyl, chlorogenic acid isopropyl, chlorogenic acid hexyl, chlorogenic acid octyl, chlorogenic acid benzyl, chlorogenic acid phenethyl, chlorogenic acid phenylpropyl, chlorogenic acid phenylbutyl, chlorogenic acid phenylisopentyl, chlorogenic acid phenylhexyl, chlorogenic acid phenyloctyl, chlorogenic acid styryl, chlorogenic acid benzyl alcohol, chlorogenic acid phenylethanol, anthocyanidin, proanthocyanidin glycoside, and catechin.;
[0222] 43. According to the water-soluble carbon chain substance described in any one of the previous technical solutions, the water-soluble carbon chain substance includes water-soluble medium and short-chain fatty acids, or fatty acid salts, or fatty acid derivatives. Preferably, for example, water-soluble medium and short-chain fatty acids such as butyric acid, succinic acid, fumaric acid, valeric acid, glutaric acid, caproic acid, adipic acid, enanthic acid, pimelic acid, caprylic acid, octenoic acid, suberic acid, capric acid, sebacic acid; and, as fatty acid derivatives including any one or more of the following, such as surfactants: fatty acid salts, alkyl sulfonates, alkyl sulfates, alkyl phosphates, alkyl amine salts, alkyl quaternary ammonium salts, aliphatic acyl amino acids, betaines, fatty alcohol polyoxyethylene ethers, alkylphenol polyoxyethylene ethers, aliphatic amine polyoxyethylene ethers, polyol fatty acid esters, polyol polyoxyethylene ether fatty acid esters, fatty acid polyoxyethylene esters, alkyl polyglucosides, and alkyl ethoxy polyglucosides. It contains one or more substances selected from the group consisting of water-soluble medium and short-chain fatty acids, or fatty acid salts, or fatty acid derivative substances.
[0223] 44. A preparation for regulating transmembrane transport of cell membranes, the structure or function of cell membranes, cell division and proliferation or cell migration and locomotion, cell aging, and / or the fluidity of cell membranes, prepared using the water-soluble carbon chain substance described in any one of the previous technical solutions.
[0224] 45. According to the preparation described in the previous technical solution, the regulation of the fluidity of the cell membrane is an improvement in the fluidity of the cell membrane.
[0225] 46. According to the preparation described in the previous technical solution, the regulation of the fluidity of the cell membrane is a decrease in the fluidity of the cell membrane.
[0226] According to the preparation described in the previous technical solution, the cell membrane includes a cytoplasmic membrane and an organelle membrane, and the cell membrane or cell includes the cell membrane or cell of a microorganism, or the cell membrane or cell of a tissue of a plant, animal or human body. The regulation includes increase or promotion, and inhibition or decrease. Here, the cell membrane of the microorganism includes the cell membranes of bacteria and fungi and the envelope of the virus. Here, the cell membrane structure includes a phospholipid bilayer, proteins adsorbed on the surface of the phospholipid bilayer, and polysaccharides embedded and inserted into the phospholipid bilayer. Specifically, it includes receptor proteins, transmembrane proteins, cytoskeletal proteins, and enzymes. Here, transmembrane transport includes active transport, passive transport, endocytosis, and exocytosis.
[0227] According to the preparation described in the previous technical solution, the regulation of the transmembrane transport of the cell membrane includes increasing and promoting the release of extracellular exosomes in the cell, and also includes suppressing or reducing the release of extracellular exosomes in the cell, and preventing the entry of viruses into the cell. The suppression or reduction of the transmembrane transport of the virus suppresses or reduces the entry of the virus into the cell through the endocytosis effect, or suppresses or reduces the entry of the virus into the cell through the fusion of the virus envelope and the cell membrane. It is used for all of the prevention of virus infection, the prevention of mycoplasma and chlamydia infection, and the prevention of bacterial infection. The substances transported through the cell membrane include at least one or two or more of small molecule compounds, medium molecule compounds, macromolecule compounds, viruses, bacteria, pathogenic microorganisms such as mycoplasma, chlamydia, and fungi, and nanoparticles and nanodrugs.
[0228] According to the preparation described in the previous technical solution, the preparation for improving the fluidity of the cell membrane among the preparations includes preparations for drug delivery, gene transfection, cell therapy, diabetes, nervous system, improvement of Alzheimer's disease, strengthening of the immune system, prevention, prevention, improvement and / or treatment of hypercholesterolemia, and / or inflammatory bowel disease.
[0229] 50. According to the formulation described in the previous technical solution, the formulation for reducing the fluidity of cell membranes among the said formulations includes formulations for the prevention, inhibition, improvement and / or treatment of cardiovascular diseases (including coronary heart disease, hypertension, myocardial infarction, heart failure), obesity, autism, osteoporosis, inflammatory diseases, autoimmune diseases, chronic fatigue syndrome, leukemia, autocytolysis, viral infections and / or neurodegenerative diseases.
[0230] 51. A formulation for preventing, inhibiting or treating microbial infections, prepared using the water-soluble carbon chain substance described in any one of the previous technical solutions.
[0231] 52. According to the formulation described in the previous technical solution, the formulation is a pharmaceutical formulation or an environmental disinfection and sterilization formulation, and the said pharmaceutical formulation is preferably one selected from inhalants, nasal sprays, injections, oral formulations, and topical skin dosage forms.
[0232] 53. The use of the water-soluble carbon chain substance described in any one of the previous technical solutions in the preparation of a pharmaceutical formulation or an environmental disinfection and sterilization microbial reagent for preventing, inhibiting and / or treating microbial infections, preferably, the said microbe is any one or two selected from viruses, bacteria, and fungi, the said virus is an enveloped virus and / or a non-enveloped virus, more preferably, the said virus is one or more viruses selected from novel coronavirus, influenza virus, human immunodeficiency virus (HIV), hepatitis B virus, human herpes virus, Ebola virus, rabies virus, and human papillomavirus (HPV), the said bacteria are one or more bacteria selected from Escherichia coli, Staphylococcus aureus, methicillin-resistant Staphylococcus aureus, Streptococcus pneumoniae, Klebsiella pneumoniae, and Pseudomonas aeruginosa, and even more preferably, the said virus is one or more selected from H7N9 influenza virus, H5N1 influenza virus, HIV virus, novel coronavirus, HPV virus and rabies virus.
[0233] According to the use described in the previous technical solution, when the water-soluble carbon chain substance described in Technical Solution 54 acts on microorganisms, it is prepared into a solution with a concentration of 0.2 mM to 10 mM.
[0234] According to the use described in the previous technical solution, it is prepared into a solution with a concentration of 0.5 mM to 10 mM.
[0235] A preparation for preventing, inhibiting or treating an inflammatory reaction and / or body aging, prepared using the water-soluble carbon chain substance described in any one of the previous technical solutions.
[0236] According to the preparation described in the previous technical solution, the prevention of body aging includes the prevention of skin aging, and the prevention, inhibition or treatment of the inflammatory reaction includes changing the three-dimensional structure of inflammatory factors (proteins).
[0237] According to the preparation described in the previous technical solution, the carbon chain substance binds to oxygen radicals.
[0238] According to the preparation described in the previous technical solution, the carbon chain substance is Flavon, Isoflavon, Anthocyanin, Soy Isoflavon, Aloesin, Grape Seed Extract, Green Tea-derived Flavon, Naringenin, Limocitrin, Baicalein, Riboflavin, Quercetin, Graphite-derived Flavon, Sinzelenanin, Chrysin, Japanese Apricot Flavon, Morin, Luteolin, Mulberry Extract, Gypsum-derived Flavon, Honeysuckle-derived Flavon, Violet-derived Flavon, Perilla-derived Flavon, Chrysanthemum-derived Flavon, Artemisinin, Red Peony-derived Flavon, Salvia-derived Flavon, Bupleurum-derived Flavon, Safflower-derived Flavon, Rock Jasmine-derived Flavon, Jujube-derived Flavon, Gynostemma-derived Flavon, Prepared Rehmannia Root-derived Flavon, Chinese Date-derived Flavon, Schisandra Chinensis-derived Flavon, Licorice-derived Flavon, Panax Ginseng-derived Flavon, Curcumin, Apigenin, Carotene, Anthocyanidin, Lutein, Zeaxanthin, Horseradish Extract, Rutin, Scutellarein, Pollen Yellow Extract, Sage-derived Flavon, Dandelion-derived Flavon, Cinnamon-derived Flavon, Isoflavonoid, and Anthocyanidin; Rutin, Emodin, Fucoxanthin, Gallic Acid, Persimmon Peel Extract, Morin, Echinacoside, Grape Seed-derived Procyanidin, Phenolic Acid, Tea Polyphenol, Naringin, Citric Acid, Flavonol, Glycyrrhizic Acid, Cinnamic Acid, Flavonoid Glycoside, Oleic Acid, Matrine, Tanshinone, Erythrophleine, Snadigmic Acid, Perillyl Alcohol, Anisic Acid, Amrencin, Hesperidin, Granatin, Morcin, Naringin, Linarin, Gentiopicroside, Jasminosid, Naringetol, Carotene, Apigenin, Baimelin, Scutellaria Baicalensis Georgi Extract, Kingoside, Chrysanthemum morifolium Ramat Extract, Olive Extract, Oolong Tea Extract, L-Theanine, Red Wine Extract, Platycodon grandiflorum A. DC. Glycoside, Perilla Alcohol Glycoside, Moracin, Calthamin, Pinosin, Pakiminic Acid, Caffeic Acid, Chlorogenic Acid; Resveratrol, White Tea Polyphenol, Resveratrol Disaccharide, Banana-derived Lutein, Anthocyanidin, Arachidonic Acid, Peanut-derived Flavon, (+)-Piperitol, Anisofolin, Flavonoid, Baicalein, Flavonoid Glycoside, Flavanol, Red Wine Polyphenol, Rodiosin, Calphenol, Black Tea-derived Flavon, Sesamin, Triticum aestivum L. Phenol, Fucitol, Seaweed Polysaccharides, Alginate, Farnesin, Cannabidiol, Polydatin,One or more substances selected from the group consisting of cucurbitacin, fenugreek extract, cucurbitic acid, pollen phenol, pollen-derived flavone, pollen glycoside, pollen ester, arachidic acid, peanut-derived flavone glycoside, peanut isoflavone, peanut isoflavone glycoside, peanut isoflavone disaccharide, peanut isoflavone trisaccharide, peanut resveratrol, peanut resveratrol disaccharide, peanut resveratrol trisaccharide, peanut resveratrol tetrasaccharide, peanut resveratrol pentasaccharide, peanut resveratrol hexasaccharide, peanut resveratrol heptasaccharide, peanut resveratrol octasaccharide, peanut resveratrol nonasaccharide, peanut resveratrol decasaccharide, peanut resveratrol undecasaccharide, catechin, epicatechin, tea polyphenol, catechol, chlorophyll, protocatechuic acid, hesperidin, anthocyanidin, anthocyanin, anthocyanin, cyanidin alcohol, glucoside, glucopyranoside, tricin, soybean isoflavone, flavanol, keltaninin, buckwheat extract, persimmon peel extract, persimmon tannic acid, punica acid, granatin, blueberry extract, resveratrol, lycopene, naringenin, morin, chlorogenic acid, chlorogenic acid triglucoside, chlorogenic acid diglucoside, chlorogenic acid methyl, chlorogenic acid ethyl, chlorogenic acid propyl, chlorogenic acid butyl, chlorogenic acid isopropyl, chlorogenic acid hexyl, chlorogenic acid octyl, chlorogenic acid benzyl, chlorogenic acid phenethyl, chlorogenic acid phenylpropyl, chlorogenic acid phenylbutyl, chlorogenic acid phenylisopentyl, chlorogenic acid phenylhexyl, chlorogenic acid phenyloctyl, chlorogenic acid styryl, chlorogenic acid benzyl alcohol, chlorogenic acid phenylethanol, anthocyanidin, proanthocyanidin glycoside, and catechin are combined, or the carbon chain substance is one or more substances selected from the group consisting of the above substances, or the carbon chain substance is mixed with one or more substances selected from the group consisting of the above substances to prepare a formulation.
[0239] According to the preparation described in any one of the previous technical solutions, when the preparation is used for the prevention, inhibition or treatment of inflammatory reactions and / or the aging of the body, the water-soluble carbon chain substance is prepared into a solution with a concentration of 0.1 nM to 5 mM. Preferably, the carbon chain substance is a complex formed by fatty acids and amino acids. More preferably, the concentration of the complex solution is 0.1 nM to 300 μM, and even more preferably 5 nM to 100 μM.
[0240] According to the preparation described in the previous technical solution, when the preparation is used for the prevention, inhibition or treatment of inflammatory reactions and / or the aging of the body, the water-soluble carbon chain substance is prepared into a solution with a concentration of 0.1 nM to 300 μM, preferably 5 nM to 100 μM.
[0241] A pharmaceutical preparation for preventing, inhibiting, alleviating or treating neurodegenerative diseases, prepared using the water-soluble carbon chain substance described in any one of the previous technical solutions.
[0242] According to the pharmaceutical preparation described in the previous technical solution, the neurodegenerative diseases include Alzheimer's disease (AD), Parkinson's disease (PD), Huntington's disease (HD), Alzheimer's disease, amyotrophic lateral sclerosis (ALS), various types of spinocerebellar ataxia (SCA), or Pick's disease.
[0243] According to the pharmaceutical preparation described in the previous technical solution, the water-soluble carbon chain substance is prepared into a solution with a concentration of 0.1 nM to 5 mM to exert its effect.
[0244] According to the pharmaceutical preparation described in the previous technical solution, the water-soluble carbon chain substance is prepared into a solution with a concentration of 0.1 nM to 300 μM, preferably 5 nM to 100 μM to exert its effect.
[0245] The preparation prepared with the carbon chain substance of the present invention is used to reduce the fluidity of cell membranes and can be applied to the following modes and diseases. 1) Cardiovascular diseases (including coronary heart disease, hypertension, myocardial infarction, heart failure): Reducing the fluidity of cell membranes can reduce the risk of heart disease and stroke. Moderately reducing the fluidity of cell membranes can reduce the burden on the heart and relieve the symptoms of cardiovascular diseases. Moderately reducing the fluidity of cell membranes can reduce the activity of sodium channels and calcium channels on the cell membrane, thereby reducing the influx of intracellular calcium ions, reducing the excitability of cardiomyocytes and the burden on the heart, and alleviating the symptoms of cardiovascular diseases. 2) Obesity: Reducing the fluidity of cell membranes is beneficial for improving fat metabolism, reducing fat accumulation, and alleviating the symptoms of obesity. 3) Autism: Reducing the fluidity of cell membranes is beneficial for improving the function of brain cells and thereby alleviating the symptoms of autism. 4) Osteoporosis: Reducing the fluidity of cell membranes can promote the growth of bone cells, improve bone density, and thereby enable the prevention and treatment of osteoporosis. 5) Inflammatory diseases: Reducing the fluidity of cell membranes can reduce the inflammatory reaction and is beneficial for controlling the symptoms of inflammatory diseases. 6) Autoimmune diseases: Moderately reducing the fluidity of cell membranes can reduce the autoimmune reaction and alleviate the symptoms of autoimmune diseases. 7) Chronic fatigue syndrome: Moderately reducing the fluidity of cell membranes can alleviate fatigue symptoms. 8) Autocytolysis: Reducing the fluidity of cell membranes can prevent the loss of intracellular substances and thereby prevent autocytolysis. 9) Neurodegenerative diseases: Reducing the fluidity of cell membranes can prevent the loss of useful substances in neurons and thereby prevent neurodegenerative diseases. 10) Prevention of viral infections, etc.: Reducing the fluidity of cell membranes can reduce the possibility of viruses invading cells and tumor cells spreading.
[0246] The preparation prepared from the carbon chain substance of the present invention can increase the permeability of the cell membrane by moderately improving the fluidity of the cell membrane, promote the passage of substances through the cell membrane, and can be applied to the following aspects and diseases. Drug delivery: For drug molecules to enter the cell interior, they need to pass through the cell membrane. However, due to the biological properties of the cell membrane, many drugs cannot pass through the cell membrane. Therefore, by improving the fluidity of the cell membrane, the passing speed of drug molecules through the cell membrane can be increased, the passing efficiency can be improved, and the drug delivery effect can be improved. Gene transfection: Similarly, improving the fluidity of the cell membrane can improve the speed and efficiency of foreign genes entering the cell interior through the cell membrane, and achieve gene transfection. Cell therapy: In some cell therapies, it is necessary to introduce foreign cells into host cells. For foreign cells to enter host cells, they need to pass through the host cell membrane. Therefore, improving the fluidity of the cell membrane can improve the efficiency of foreign cells passing through the host cell membrane. Tumor treatment: By improving the fluidity of the cell membrane, the speed of chemotherapeutic drugs entering tumor cells through the cell membrane can be increased, the efficiency can be improved, and thereby the therapeutic effect of chemotherapeutic drugs can be improved. Diabetes: Diabetic patients often have lower cell membrane fluidity compared to healthy individuals. By reducing the fluidity of the cell membrane, insulin sensitivity can be increased, which is helpful for controlling blood sugar levels. Improvement of neurological diseases: The water-soluble fatty acid complex can improve the symptoms of neurological diseases by improving the fluidity of the cell membrane and promoting the regeneration of nerve cells. Alzheimer's disease: A decrease in cell membrane fluidity may lead to nerve cell death, but by improving the fluidity of the cell membrane, nerve cell death can be reduced. Enhancement of the immune system: A decrease in cell membrane fluidity may lead to a decrease in the function of the immune system. By improving the fluidity of the cell membrane, the function of the immune system can be enhanced, which is helpful for preventing infections and diseases. Leukemia: Leukemia is a type of cancer caused by abnormal proliferation of white blood cells. A water-soluble fatty acid complex that improves the fluidity of the cell membrane may make it easier for chemotherapeutic drugs to penetrate into white blood cells, thereby potentially improving the therapeutic effect. Hypercholesterolemia: Hypercholesterolemia may cause arteriosclerosis and cardiovascular diseases. The water-soluble fatty acid complex improves the fluidity of the cell membrane and helps reduce blood cholesterol levels. Inflammatory bowel disease: Inflammatory bowel disease is a chronic inflammatory bowel disease including Crohn's disease and ulcerative colitis. Some studies have shown that the water-soluble fatty acid complex can reduce intestinal inflammation by improving the fluidity of the intestinal epithelial cell membrane.
[0247] By moderately improving the fluidity of the cell membrane, the permeability of the cell membrane can be increased, promoting the passage of substances through the cell membrane, and it can be applied to the following aspects and diseases. Drug delivery: For drug molecules to enter the cell interior, they need to pass through the cell membrane. However, due to the biological properties of the cell membrane, many drugs cannot pass through the cell membrane. Therefore, by improving the fluidity of the cell membrane, the speed and efficiency of drug molecules passing through the cell membrane can be increased, improving the drug delivery effect. Gene transfection: Similarly, improving the fluidity of the cell membrane can increase the speed and efficiency of foreign genes entering the cell through the cell membrane, achieving gene transfection. Cell therapy: In some cell therapies, it is necessary to introduce foreign cells into host cells. For foreign cells to enter host cells, they need to pass through the host cell membrane. Therefore, improving the fluidity of the cell membrane can increase the efficiency of foreign cells passing through the host cell membrane. Tumor treatment: By improving the fluidity of the cell membrane, the speed and efficiency of chemotherapeutic drugs entering tumor cells through the cell membrane can be increased, thereby improving the therapeutic effect of chemotherapeutic drugs. Diabetes: Diabetic patients often have lower cell membrane fluidity compared to healthy individuals. By reducing the fluidity of the cell membrane, insulin sensitivity is enhanced, which helps in controlling blood sugar levels. Improvement of neurological diseases: The water-soluble fatty acid complex can improve the symptoms of neurological diseases by enhancing the fluidity of the cell membrane and promoting the regeneration of nerve cells. Alzheimer's disease: A decrease in cell membrane fluidity may lead to nerve cell death, but by improving the fluidity of the cell membrane, nerve cell death can be reduced. Enhancement of the immune system: A decrease in cell membrane fluidity may lead to a decline in the function of the immune system. By improving the fluidity of the cell membrane, the function of the immune system can be strengthened, which helps in preventing infections and diseases. Leukemia: Leukemia is a type of cancer caused by the abnormal proliferation of white blood cells. The water-soluble fatty acid complex that improves the fluidity of the cell membrane may make it easier for chemotherapy drugs to penetrate into white blood cells, thereby potentially improving the treatment effect. Hypercholesterolemia: Hypercholesterolemia may cause arteriosclerosis and cardiovascular diseases. The water-soluble fatty acid complex improves the fluidity of the cell membrane and helps in reducing blood cholesterol levels. Inflammatory bowel disease: Inflammatory bowel disease is a group of chronic inflammatory bowel diseases such as Crohn's disease and ulcerative colitis.
[0248] The carbon chain substance of the present invention affects the structure and function of cell membranes, increases or suppresses transmembrane substance transport of cell membranes, improves or decreases the fluidity of cell membranes, increases or suppresses cell division, increases or suppresses cell migration, and affects cell aging and the like. The water-soluble carbon chain substance originally contains a carbon chain having a certain water solubility, and its structure includes at least one or more hydrophobic carbon chain portions and one or more hydrophilic groups or residues, and also includes a hydrophilic complex formed by coupling the hydrophobic carbon chain portion to a water-soluble molecule. The water-soluble carbon chain can be used for the prevention and treatment of viral, bacterial and fungal infections, anti-aging, prevention and reduction of the onset of neurodegenerative diseases such as Alzheimer's disease, and by reducing the non-specific phagocytosis of nanodrugs by cells, the nanodrug action at the target lesion is enhanced.
[0249] The present invention has experimentally shown in advance that when the water-soluble fatty acid complex of the present invention functions as a water-soluble carbon chain substance, its concentration range can be controlled with reference to the following concentration and mechanism explanations. (1) Concentration range of the water-soluble fatty acid complex acting on cells: 0.1 nM to 5 mM, preferably 1 nM to 0.3 mM, and a more preferred range is 5 nM to 0.1 mM. Those skilled in the art can understand the blood drug concentration range acting on animals or humans with reference to this experimental concentration range. (2) Concentration range for suppressing cell membrane fluidity: The action range of each water-soluble fatty acid complex is different from that of other water-soluble fatty acid complexes. For most water-soluble fatty acid complexes, the concentration for suppressing cell membrane fluidity is from 0.1 nM to 30 micromoles. A decrease in cell membrane fluidity may lead to the following diseases. 1) Hypertension: A decrease in cell membrane fluidity in hypertensive patients may be related to abnormal functions of vascular endothelial cells. 2) Diabetes: A decrease in cell membrane fluidity in diabetic patients may be related to oxidative stress caused by hyperglycemia and the formation of advanced glycation end products. 3) Heart disease: A decrease in cell membrane fluidity in heart disease patients may be related to structural and functional abnormalities of myocardial cell membranes. 4) Autoimmune diseases: A decrease in cell membrane fluidity in autoimmune disease patients may be related to abnormal activation of the immune system and inflammatory responses. The above diseases can be treated by appropriately improving cell membrane fluidity. (3) When cell membrane fluidity decreases, transmembrane transport of substances, including transmembrane transport of macromolecules, small molecules, and particulate substances, is restricted and inhibited. (4) Concentration range for improving cell membrane fluidity: The action range of each water-soluble fatty acid complex is different from that of other water-soluble fatty acid complexes. Generally, at a concentration from 50 micromoles to 500 micromoles, cell membrane fluidity is improved. (5) Physiological and pathological processes corresponding to the improvement of cell membrane fluidity include the following. When cell membrane fluidity is improved, cells are more likely to divide and proliferate. One of the reasons is that the cell membrane fluidity is higher than that of normal cells. Cell deformation and migration are also closely related to cell membrane fluidity. For example, the chemotaxis of white blood cells is also due to high fluidity. The chemotactic ability of white blood cells to the inflammatory region also decreases. (6) When cell membrane fluidity is improved to a certain extent and the cell membrane changes from the liquid crystal state to the liquid state, the cell membrane ruptures, and the concentration of the water-soluble fatty acid at this time generally becomes 500 micromoles or more. (7) Concentration range of water-soluble fatty acid complexes that affect transmembrane transport of substances: All water-soluble fatty acid complexes affect transmembrane transport of substances, such as increasing or suppressing transmembrane transport. For example, the entry of a virus into a cell is transmembrane transport, and the secretion of insulin outside the cell via exosomes is also transmembrane transport. (8) One of the important reasons currently hindering the wide application of nanodrugs is that when these nanodrugs are injected into the body, they are phagocytosed by the phagocytic cell system and reticuloendothelial system related to the body's natural immunity. This is a protective mechanism. However, a sufficient amount of nanodrugs cannot reach the target lesion area. The water-soluble fatty acid complex suppresses the non-specific internal migration of nanodrugs by the reticuloendothelial system, enabling more nanodrugs to reach the target lesion. (9) The concentration range for suppressing aging is 5 nM to 100 μM, and the concentration range for killing microorganisms is 0.2 mM to 10 mM.
[0250] Compared with the prior art, the present invention has the following beneficial effects. 1) The water-soluble carbon chain substance according to the present invention affects the transmembrane transport of substances, cell division and proliferation, cell movement and migration, and cell aging by affecting the fluidity of the cell membrane. 2) The water-soluble carbon chain substance according to the present invention improves the fluidity of the cell membrane. When the fluidity of the cell membrane improves to a certain level, the cell changes from a liquid crystal state to a liquid state, and the cell membrane ruptures. Lipid envelopes that can destroy pathogenic microorganisms include enveloped viruses, bacteria, and fungi, and pathogenic microorganisms include enveloped viruses, bacteria, and fungi. 3) The water-soluble carbon chain substance according to the present invention affects the fluidity of the cell membrane by changing the composition, function, and structure of the cell membrane. 4) The water-soluble carbon chain substance according to the present invention binds to the proteins of the cell membrane phospholipid bilayer within a certain concentration range and changes its three-dimensional structure, thereby affecting the deformation ability of the protein, affecting its movement within the phospholipid bilayer, and resulting in a decrease in the fluidity of the cell membrane. 5.) The water-soluble carbon chain substance according to the present invention binds to endocytosis-related proteins, receptor proteins, and cytoskeletal proteins of the cell membrane lipid bilayer within a certain concentration range, changes their three-dimensional structure, suppresses the deformation ability of the proteins, and thereby can suppress the transmembrane transport ability of the substance. For example, it can prevent viruses and nano-drugs from being taken into cells. Thereby, virus infection can be prevented, non-specific phagocytosis of nano-drugs can be suppressed, and the ability to act on target lesions can be enhanced. 6) The water-soluble carbon chain substance according to the present invention binds to endocytosis-related proteins, receptor proteins, and cytoskeletal proteins of the cell membrane lipid bilayer within a certain concentration range, changes their three-dimensional structure, suppresses the deformation ability of the proteins, and thereby can suppress the transmembrane transport ability of the substance. For example, it can prevent endocytosis into the cells of bacteria and fungi. Thereby, infection by bacteria and fungi can be prevented. 7) The water-soluble carbon chain substance according to the present invention can prevent virus infection by acting on host cells, and can prevent virus infection without eliminating the virus in the host body. 8) The water-soluble carbon chain substance according to the present invention acts on cytoskeletal proteins within a certain concentration range, changes their three-dimensional structure, suppresses the deformation ability of the proteins, and thereby can suppress the movement and deformation ability of cells, and can be used for the inflammatory reaction syndrome caused by leukocyte migration in severe inflammation. 9) The water-soluble carbon chain substance according to the present invention suppresses the movement and deformation ability of cells by reducing the fluidity of the cell membrane within a certain concentration range. It can be used for the inflammatory reaction syndrome caused by leukocyte migration in severe inflammation. 10) The water-soluble carbon chain substance according to the present invention can suppress cell aging by improving the fluidity of the cell membrane within a certain concentration range, and can be used to resist the aging of the body and the skin. 11) The water-soluble carbon chain substance according to the present invention binds to oxygen radicals, changes the three-dimensional structure of inflammatory factors (proteins), suppresses the inflammatory reaction, and has an anti-inflammatory effect and an anti-aging effect. On the other hand, the water-soluble carbon chain substance stabilizes the cell membrane by reducing the fluidity of the cell membrane within a certain concentration range, suppresses the rupture of the cell membrane caused by the action of inflammatory factors, releases more inflammatory factors inside the cell, and suppresses the occurrence of inflammation.
Brief Description of Drawings
[0251]
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Embodiments for Carrying Out the Invention
[0252] The present invention aims to provide a water-soluble carbon chain substance that affects the transmembrane substance transport, membrane fluidity, membrane structure and function of cell membranes. The carbon chain substance may be a compound, a complex or a mixture. 1.1. The water-soluble carbon chain substance includes: a. a carbon chain that originally has a certain water solubility and whose structure includes at least one or more hydrophobic carbon chain portions and one or more hydrophilic groups or residues; b. a highly hydrophilic complex formed by covalently bonding the hydrophobic carbon chain portion to a water-soluble molecule. 1.2. The water-soluble carbon chain substance affects the structure and function of cell membranes, affects the transmembrane substance transport of cell membranes, affects cell division and proliferation, affects cell movement and migration, affects the fluidity of cell membranes, and affects cell aging. 1.3. The effects include increase and promotion, or inhibition and decrease. 1.4. The water-soluble carbon chain substance shows an increasing and promoting effect within a certain concentration range of the same water-soluble carbon chain, and shows an inhibitory and decreasing effect within another concentration range. 1.5. The cell membranes include cytoplasmic membranes and organelle membranes, and include cell membranes of humans, animals, plants, bacteria and fungi, and envelopes of viruses. 1.6. The cell membrane structure includes a phospholipid bilayer, proteins adsorbed on the surface of the phospholipid bilayer, and polysaccharides embedded and inserted into the phospholipid bilayer, including receptor proteins, transmembrane proteins, cytoskeletal proteins, and enzymes. 1.7. The effect on the function of cell membranes affects the transmembrane transport function of cell membranes, that is, it includes increasing and promoting, or inhibiting or decreasing the transmembrane transport function of cell membranes. The transmembrane transport includes the functions of active transport, passive transport, endocytosis and exocytosis. 1.7.1. The active transport includes the Na+-K+ pump and the Ca2+ pump, ATP-driven pump transport including the P class, V class, F class, and ABC superfamily class, and cotransport. The passive transport includes simple diffusion and facilitated diffusion. The endocytosis includes phagocytosis, exocytosis, and receptor-mediated endocytosis. 1.8. In the function of suppressing or reducing transmembrane transport, the transmembrane transport substances include small molecule compounds, medium molecule compounds, macromolecule compounds, pathogenic microorganisms such as viruses, bacteria, mycoplasma, chlamydia, and fungi, and nanoparticles and nano drugs. 1.9. The suppression or reduction of the transmembrane transport of the virus suppresses or reduces the entry of the virus into the cell through the endocytosis effect, or suppresses or reduces the entry of the virus into the cell through the fusion of the virus envelope and the cell membrane, and is used for all prevention of virus infection. The suppression or reduction of the transmembrane transport of the mycoplasma, chlamydia, bacteria, and fungi can be used for the prevention of mycoplasma and chlamydia infections and the prevention of bacterial and fungal infections. 1.10. The suppression or reduction of the transmembrane transport of the nanoparticles or nano drugs suppresses or reduces the entry of the nanoparticles or nano drugs into the cell through the endocytosis effect, can prevent, suppress, or reduce the non-specific phagocytosis of the nanoparticles or nano drugs by the cells, thereby enabling more nano drugs to enter the target site and improving the effective utilization of the nano drugs. 1.11. The influence on the transmembrane transport of the cell membrane includes an increase and promotion of the release of exosomes in the cell to the outside of the cell, and also includes the suppression or reduction of the release of exosomes in the cell to the outside of the cell. 1.12. The influence on the structure and function of the cell membrane includes affecting the fluidity of the cell membrane, and promoting the growth and division of the cell by increasing the fluidity of the cell membrane. 1.13. The increase in the fluidity of the cell membrane changes the phospholipid bilayer in the cell membrane from the liquid crystal state to the liquid state by increasing the fluidity of the cell membrane, resulting in the rupture of the cell membrane. 1.14. The increase in the fluidity of the cell membrane is used to disrupt the lipid envelopes of viruses, mycoplasmas, chlamydias, bacteria, and fungi that have lipid envelopes by increasing the fluidity of the cell membrane, causing the phospholipid bilayer in the cell membrane to change from the liquid crystal state to the liquid state, resulting in the rupture of the cell membrane, and is used for the treatment of infections by viruses, mycoplasmas, chlamydias, bacteria, and fungi. 1.15. The decrease in the fluidity of the cell membrane maintains the stability of the membrane, reduces cell division and proliferation, reduces and suppresses the release of intracellular inflammatory factors due to cell membrane rupture, thereby reducing the inflammatory reaction and degree, and thereby has the effects of preventing aging, prolonging life, and preventing skin aging in humans and other animals. 1.16. The suppression or reduction of the entry of viruses, bacteria, and mycoplasmas into cells through endocytosis or membrane fusion can be used for the prevention of viral diseases and other pathogenic microorganism infections, and further includes chronic diseases caused by viral, bacterial, and mycoplasma infections: neurodegenerative diseases including Alzheimer's disease (AD), Parkinson's disease (PD), Huntington's disease (HD), Alzheimer's disease, amyotrophic lateral sclerosis (ALS), various types of spinocerebellar ataxia (SCA), Pick's disease, etc.; degenerative nerve disorders including degenerative nerve disorders caused by intracranial nerve infections by herpes virus. 1.17. The influence on the function of the cell membrane further includes affecting cell movement and migration, including promoting or suppressing the movement of macrophages and immune cells, promoting or suppressing the migration and movement of melanocytes, and promoting or suppressing the migration and movement of hair follicle cells. 1.18 The reduction in the fluidity of the cell membrane and the suppression of the ability of cells to move and deform are used for the inflammatory reaction syndrome caused by the migration of white blood cells in severe inflammation, reducing the fluidity of the cell membrane to stabilize the cell membrane, suppressing the rupture of the cell membrane caused by the action of inflammatory factors, and suppressing the occurrence of inflammation. 1.19 The increase in the fluidity of the cell membrane can suppress cell aging and is used for preventing body aging and skin aging. 1.20 The above-mentioned group of water-soluble carbon chain substances can change the three-dimensional structure of inflammatory factors (proteins) by binding to oxygen radicals, further suppress the inflammatory reaction, and further have anti-inflammatory and anti-aging effects.
[0253] 2. Structural composition of water-soluble carbon chain substances In the present invention, the "water-soluble carbon chain" or "carbon chain" includes two cases of substances or residues having a carbon chain. The "water-soluble carbon chain substance" or "carbon chain substance" is a substance (which may be a molecule) containing a carbon chain or a carbon chain residue or a carbon chain moiety, or a complex or physical mixture of the substance (which may be a molecule) and a molecule or residue containing other hydrophilic groups. That is, in some cases, the water-soluble carbon chain substance in the present invention is itself a compound, a residue having both a hydrophilic group and a hydrophobic carbon chain moiety or a carbon chain. In some cases, the water-soluble carbon chain substance is an aliphatic hydrocarbon, fatty acid, aliphatic alcohol or ether or ester or surfactant or various derivatives thereof having a carbon chain (preferably a carbon chain having 3 to 100 carbon atoms), or a carbon chain residue of these carbon chain substances themselves, and a compound or complex obtained by reacting with at least one selected from other substances such as proteins, polypeptides, oligopeptides, oligosaccharides, monosaccharides, disaccharides, nucleotides, vitamins, amino acids, water-soluble polymers, water-soluble polyamino acids and polysaccharide molecules, or a mixture of the unreacted carbon chain residue or carbon chain substance and / or the unreacted protein, polypeptide, oligopeptide, oligosaccharide, monosaccharide, disaccharide, nucleotide, vitamin, amino acid, water-soluble polymer, water-soluble polyamino acid and / or polysaccharide molecule. 2.1. The carbon chain moiety having a certain water solubility has a polar group or residue having water solubility in the molecule, such as a hydroxy group, carboxyl group, amino group, amine group, quaternary ammonium group, guanidino group, mercapto group, sulfonic acid group, sulfonyloxy group, phosphate group, and the number of carbon atoms constituting the carbon chain is 3 to 100. 2.1.1. Carbon chain substances with a certain water solubility include medium- and short-chain fatty acids with lower water solubility themselves, such as acetic acid, oxalic acid, propionic acid, lactic acid, pyruvic acid, citric acid, butyric acid, succinic acid, malic acid, tartaric acid, fumaric acid, valeric acid, glutaric acid, caproic acid, adipic acid, enanthic acid, pimelic acid, caprylic acid, octenoic acid, suberic acid, decanoic acid, sebacic acid, and fatty acid derivatives including surfactants: fatty acid salts, alkyl sulfonates, alkylbenzene sulfonates, alkyl sulfate esters, alkyl phosphate esters, alkylamine salts, alkyl quaternary ammonium salts, aliphatic acyl amino acids, betaines, fatty alcohol polyoxyethylene ethers, alkylphenol polyoxyethylene ethers, aliphatic amine polyoxyethylene ethers, polyol fatty acid esters, polyol polyoxyethylene ether fatty acid esters, fatty acid polyoxyethylene esters, alkyl polyglucosides, alkyl ethoxypolyglucosides. The water-soluble carbon chain substances of the present invention are small molecule compounds containing hydroxy groups and benzene rings: Flavon, Isoflavon, Anthocyanin, Soy Isoflavon, Aloe-emodin, Grape Seed Extract, Green Tea-derived Flavon, Naringenin, Limocitrin, Baicalein, Riboflavin, Quercetin, Graphite-derived Flavon, Shinzelanin, Chrysin, Japanese Apricot Flavon, Morin, Luteolin, Mulberry Extract, Gypsum-derived Flavon, Honeysuckle-derived Flavon, Gentoflavin, Platycodon-derived Flavon, Violet-derived Flavon, Perilla-derived Flavon, Chrysanthemum-derived Flavon, Artemisinin, Red Peony-derived Flavon, Salvia-derived Flavon, Bupleurum-derived Flavon, Safflower-derived Flavon, Rock Jasmine-derived Flavon, Chinese Date-derived Flavon, Chinese Wolfberry-derived Flavon, Prepared Rehmannia Root-derived Flavon, Jujube-derived Flavon, Schisandra Chinensis-derived Flavon, Licorice-derived Flavon, Sanchi-derived Flavon, Curcumin, Apigenin, Carotene, Anthocyanidin, Lutein, Zeaxanthin, Horseradish Extract, Rutin, Scutellarein, Pollen Yellow Extract, Sage-derived Flavon, Dandelion-derived Flavon, Cinnamon-derived Flavon, Isoflavonoid, and Anthocyanidin; Rutin, Emodin, Fucoxanthin, Gallic Acid, Persimmon Peel Extract, Morin, Echinacoside, Grape Seed-derived Procyanidin, Phenolic Acid, Tea Polyphenol, Naringin, Citric Acid, Flavonol, Glycyrrhizic Acid, Cinnamic Acid, Flavonoid Glycoside, Oleic Acid, Matrine, Tanshinone, Erythrophleine, Snadigmic Acid, Perillyl Alcohol, Anisic Acid, Amrencin, Hesperidin, Granatin, Morsin, Naringin, Linarin, Gentiopicroside, Jasminosid, Naringetol, Carotene, Apigenin, Baimelin, Sophora Japonica Extract, King Side, Chrysanthemum Extract, Olive Extract, Oolong Tea Extract, L-Theanine, Red Wine Extract, Platycodon Glycoside, Perilla Alcohol Glycoside, Moracin, Calthamin, Pinosin, Pakiminic Acid, Caffeic Acid, Chlorogenic Acid;Resveratrol, white tea polyphenols, resveratrol disaccharide, banana-derived lutein, anthocyanidin, arachidonic acid, peanut-derived flavone, (+)-piperitol, anisofolin, flavonoid, baicalein, flavone glycoside, flavanol, red wine polyphenols, rhodiocyan, calphenol, black tea-derived flavone, sesamin, rye wheat phenol, fucitol, seaweed polysaccharides, alginic acid, farnesin, cannabidiol, polydatin, cucurbitacin, fenugreek extract, cucurbitic acid, pollen phenol, pollen-derived flavone, pollen glycoside, pollen ester, arachidonic acid, peanut-derived flavone glycoside, peanut isoflavone, peanut isoflavone glycoside, peanut isoflavone disaccharide, peanut isoflavone trisaccharide, peanut resveratrol, peanut resveratrol disaccharide, peanut resveratrol trisaccharide, peanut resveratrol tetrasaccharide, peanut resveratrol pentasaccharide, peanut resveratrol hexasaccharide, peanut resveratrol heptasaccharide, peanut resveratrol octasaccharide, peanut resveratrol nonasaccharide, peanut resveratrol decasaccharide, peanut resveratrol undecasaccharide, catechin, epicatechin, tea polyphenols, catechol, chlorophyll, protocatechin, hesperidin, anthocyanidin, anthocyanin, anthocyanin, cyanidin alcohol, glucoside, glucopyranoside, tricin, soybean isoflavone, flavanol, keltaninin, dattansoba extract, persimmon peel extract, persimmon tannic acid, punica acid, granatin, blueberry extract, resveratrol, lycopene, naringenin, morin, chlorogenic acid, chlorogenic acid triglucoside, chlorogenic acid diglucoside, chlorogenic acid methyl, chlorogenic acid ethyl, chlorogenic acid propyl, chlorogenic acid butyl, chlorogenic acid isopropyl, chlorogenic acid hexyl, chlorogenic acid octyl, chlorogenic acid benzyl, chlorogenic acid phenethyl, chlorogenic acid phenylpropyl, chlorogenic acid phenylbutyl, chlorogenic acid phenylisopentyl, chlorogenic acid phenylhexyl, chlorogenic acid phenyloctyl, chlorogenic acid styryl, chlorogenic acid benzyl alcohol, chlorogenic acid phenylethanol, anthocyanidin, proanthocyanidin glycoside, and contains some catechin.; 2.2. The complex formed by the hydrophobic carbon chain substance or carbon chain moiety and the water-soluble molecule is a complex formed by directly bonding the hydrophobic carbon chain to the water-soluble molecule through a chemical bond or bonding the hydrophobic carbon chain to the water-soluble molecule through a linker. 2.2.1. The hydrophobic carbon chain substance or carbon chain moiety is a molecule or residue of a molecule having 3 to 100 carbon atoms. 2.2.2. The carbon chain is saturated or unsaturated, the unsaturated bond is a double bond or a triple bond, and the number of unsaturated bonds is one or more than two. 2.2.3. The carbon chain substance or carbon chain moiety is a linear, cyclic carbon chain, or a carbon chain having a linear branch or a linear cyclic structure, or a linear or cyclic carbon chain containing oxygen, sulfur, or nitrogen heteroatoms. 2.2.4. The cyclic carbon chain - water-soluble carbon chain substance includes monocyclic rings and polycyclic rings. 2.3. The hydrophobic carbon chain substance or carbon chain moiety is a carbon chain substance or residue of a carbon chain having 3 to 100 carbon atoms selected from saturated and / or unsaturated aliphatic hydrocarbons, saturated and / or unsaturated aliphatic alcohols or oxoaliphatic alcohols, saturated and / or unsaturated fatty acids, saturated and / or unsaturated hydroxy group fatty acids, saturated and / or unsaturated oxo group fatty acids, hydrophobic amino acids, fat-soluble vitamins, carotenoids, sterols and steroid lipids, fatty acid glycerides, phospholipids, sphingomyelins, glycolipids and / or surfactants. 2.3.1. The saturated and / or unsaturated fatty acids have 3 to 50 carbon atoms. 2.3.2. The saturated and / or unsaturated fatty acids have 3 to 26 carbon atoms. 2.3.3. The saturated and / or unsaturated fatty acids are one or more fatty acids selected from acetic acid, oxalic acid, propionic acid, lactic acid, pyruvic acid, citric acid, butyric acid, succinic acid, malic acid, tartaric acid, crotonic acid, fumaric acid, valeric acid, glutaric acid, caproic acid, hexenoic acid, adipic acid, enanthic acid, heptenoic acid, pimelic acid, caprylic acid, octenoic acid, suberic acid, nonanoic acid, decanoic acid, sebacic acid, undecanoic acid, undecylenic acid, dodecanoic acid, dodecenoic acid, dodecanedioic acid, tridecanoic acid, tridecanedioic acid, tetradecanoic acid, pentadecanoic acid, pentadecanedioic acid, hexadecanoic acid, 2-hexadecenoic acid, hexadecanedioic acid, octadecanoic acid, octadecenoic acid, octadecadienoic acid, octadecatrienoic acid, octadecanedioic acid, eicosanoic acid, eicosapentaenoic acid, docosanoic acid, docosenoic acid, docosahexaenoic acid, docosandioic acid, tetracosanoic acid, triacontenoic acid, hexatriacontanoic acid. 2.3.4. The hydrophobic carbon chain substances include fatty acid ozonation products: fatty acid peroxides, hydroxy group fatty acids, oxo group fatty acids, fatty acid dicarboxylic acids, fatty aldehydes, aliphatic alcohols, and fatty acid esters. 2.4. The water-soluble part is a molecule or a residue of a molecule that is soluble in water. 2.4.1. The molecules of the water-soluble part contain one or more functional groups selected from amide groups, phosphoryloxy groups, carboxylic acid groups, phosphate groups, sulfonic acid groups, sulfonyloxy groups, hydroxy groups, quaternary ammonium groups, thioether groups, disulfide bonds, ether groups, mercapto groups, aldehyde groups, ester groups, amine groups, amino groups, urea groups, and guanidino groups. 2.4.2. The water-soluble molecules are one or more water-soluble macromolecules or their residues selected from proteins, polysaccharides, nucleic acids, and artificially synthesized water-soluble polymers, and / or one or more medium molecules or their residues selected from polypeptides, oligopeptides, oligosaccharides, oligonucleotides, and artificially synthesized medium molecular weight water-soluble polymers, and / or one or more water-soluble small molecules selected from amino acids, monosaccharides, disaccharides, nucleotides, deoxyribonucleotides, and water-soluble vitamins, or residues thereof. 2.4.3. The protein that is the water-soluble macromolecule is one or more water-soluble macromolecules selected from serum albumin, immunoglobulins, water-soluble collagen, chaperones, and water-soluble glycoproteins, The polysaccharide that is the water-soluble macromolecule is one or more water-soluble macromolecules selected from glucan, hyaluronic acid, sialic acid, heparin sulfate, heparan sulfate, chondroitin sulfate, dermatan sulfate, keratan sulfate, acetylated water-soluble cellulose derivatives, β-cyclodextrin and its derivatives, and water-soluble chitosan derivatives, The water-soluble polymer that is the water-soluble macromolecule is one or more water-soluble macromolecules selected from polyethylene glycol and carboxylated or aminated polyethylene glycol, polyvinyl alcohol and carboxylated or aminated polyvinyl alcohol, polyacrylic acid, and ammonium polyacrylate, The medium molecular weight water-soluble polymer is one or more substances selected from polypeptides, oligopeptides, oligosaccharides, oligonucleotides, and / or water-soluble polyamino acids, The water-soluble small molecule monosaccharides and / or disaccharides are one or more selected from glucose, fructose, rhamnose, sorbose, sucrose, maltose, lactose, and trehalose, The nucleotides and / or deoxyribonucleotides that are the water-soluble small molecules are selected from adenylate, guanylate, uridylate, cytidylate, thymidylate, inosine, deoxyadenylate, deoxyguanylate, deoxycytidylate, deoxythymidylate, and the water-soluble small molecule amino acids are one or more selected from serine, threonine, cysteine, asparagine, glutamine, tyrosine, lysine, arginine, histidine, aspartic acid, glutamic acid, citrulline, ornithine, taurine, and aminobutyric acid, The vitamin, which is the water-soluble small molecule, is one or more selected from vitamin B1, folic acid, pantothenic acid, vitamin B6, vitamin C, and biotin. The water-soluble proteins and polypeptides include any one of proteins that specifically target microbial lipid membranes, cell walls of bacteria and fungi, protein domains of viral surface proteins, or neutralizing antibody fragments. The water-soluble polyamino acids are any one selected from polyglutamic acid, polylysine and / or polyaspartic acid, and oligopeptides, oligosaccharides, and oligonucleotides.
[0254] 3. The water-soluble carbon chain affects the structure and function of cell membranes. 3.1. The structure and components of the phospholipid bilayer of the cell membrane: It includes a phospholipid bilayer composed of lecithin, sphingomyelin, and cholesterol, also includes a lipid raft structure, and includes the inner leaflet and outer leaflet of the phospholipid bilayer. 3.2. The structure of the cell membrane is related to proteins involved in cell endocytosis and exocytosis functions: membrane proteins of the cell membrane, transmembrane proteins of the cell membrane, receptors of the cell membrane, and cytoskeletal proteins. 3.3. The structure of the cell membrane includes glycoproteins and lipoproteins on the cell membrane surface, and polysaccharides on the cell membrane surface. 3.4. The proteins related to cell endocytosis and exocytosis functions: 3.4.1. Cell endocytosis proteins: 3.4.1.1. Clathrin proteins: Clathrin Heavy Chain 1 (CHC1), Clathrin Heavy Chain 2 (CHC2), Clathrin Light Chain A (CLTA), Clathrin Light Chain B (CLTB); 3.4.1.2. Caveolin proteins: Caveolin-1 (CAV1), Caveolin-2 (CAV2), Caveolin-3 (CAV3); 3.4.1.3. Dynamin proteins: Dynamin1, Dynamin2, Dynamin3, Dynamin-like protein (DNM1L, also known as Drp1), Dynamin-like protein 2 (DNM2); 3.4.1.4. Rab proteins: Rab1, Rab2, Rab5, Rab7, Rab11, Rab27, Rab35; 3.4.1.5. SNARE proteins: SNARE proteins: VAMP2, VAMP3, VAMP4, Syntaxin, SNAP-25, Munc18, Munc13, SNAP23; 3.4.1.6. Arf (ADP-ribosylation factor): Arf1, Arf2, Arf3, Arf6; 3.4.1.7. Bridging integrator proteins: AP180 / CALM, Epsin, EHD (Eps15 Homology Domain), Dab2 (Disabled-2); 3.4.2. Cytoskeletal proteins related to cellular endocytosis: 3.4.2.1. Actin: α-actin (Alpha-actin), β-actin (Beta-actin), γ-actin (Gamma-actin); 3.4.2.2. Tubulin: α-tubulin (Alpha-tubulin), β-tubulin (Beta-tubulin), γ-tubulin (Gamma-tubulin); 3.4.2.3. Intermediate filaments: Keratin, Myosin, Neurofilament, Glial fibrillary acidic protein (GFAP), Nuclear lamins; 3.4.2.4. Myosin: Muscle Myosin, Non-muscle Myosin, Adhesion Myosin, Neural Myosin, Cardiac Myosin: 3.4.2.5. Septin proteins: SEPT2 subtype, SEPT3 subtype, SEPT4 subtype, SEPT5 subtype, SEPT6 subtype, SEPT7 subtype, SEPT9 subtype, SEPT11 subtype; 3.4.3. Cell membrane receptor proteins related to cell endocytosis: 3.4.3.1. High-density lipoprotein receptor (HDL receptor): SR-BI, CD36, ABCA1, SR-BII, CLA-1, GPIHBP1; 3.4.3.2. LDL receptor (LDLR): LDLR-A, LDLR-B, LDLR-related protein (LRP), LDLR-related protein 1B (LRP1B), sortilin; 3.4.3.3. Transferrin receptor: Transferrin receptor 1 (TfR1), Transferrin receptor 2 (TfR2); 3.4.3.4. EGF receptor (EGFR): EGFR (ErbB1), ErbB2 (HER2), ErbB3 (HER3), ErbB4 (HER4); 3.4.3.5. TLR receptor (Toll-like receptor): TLR1, TLR2, TLR3, TLR4, TLR5, TLR6, TLR7, TLR8, TLR9, TLR10; 3.4.3.6.G Protein-Coupled Receptor (GPCR): Rhodopsin-like GPCR family, Secretin-like GPCR family, Metabotropic glutamate GPCR family, Adhesion GPCR family, Frizzled / Smoothened GPCR family; 3.4.3.7.Scavenger Receptor: Class A Scavenger Receptor, Class B Scavenger Receptor, Class C Scavenger Receptor, Class D Scavenger Receptor; 3.4.3.8.VLDL Receptor: VLDLR, LRP8; 3.4.3.9.LRP (Low-Density Lipoprotein Receptor-Related Protein) Receptor: LRP1, LRP2, LRP4, LRP5; 3.4.3.10.Chloride Ion Channel Receptor: GABA-A Receptor, GlyR Receptor, CFTR (Cystic Fibrosis Transmembrane Conductance Regulator), CLC family, Bestrophin, Anoctamin; 3.4.11.Endoglin Receptor: CD105, CD105a; 3.4.12.CD44 Protein: CD44s, CD44v; 3.5.Proteins Related to Cellular Exocytosis: Cathepsin, Tumor Necrosis Factor (TNF), Vascular Endothelial Growth Factor (VEGF), Glutathione S-Transferases (GGSTs), Tissue Inhibitors of Metalloproteinases (TIMPs), Alpha-2-Macroglobulin, Tyrosine Kinase Receptors (TKRs), G Protein-Coupled Receptors (GPCRs), Toll-Like Receptors (TLRs), Integrins, Fibrillin, Collagen, Heparan Sulfate Proteoglycans, Syndecan;
[0255] 4. Use of the function of the water-soluble carbon chain in influencing transmembrane transport in cell membranes 4.1. In the above function of inhibiting or reducing transmembrane transport, substances of cell transmembrane transport include small molecule compounds, medium molecule compounds, large molecule compounds, viruses, bacteria, pathogenic microorganisms such as mycoplasma chlamydia, and nanoparticles and nanodrugs. 4.1.1. The small molecule compound is water, glucose, amino acids, ions, O 2 , CO 2 , N 2 Includes. 4.1.2. The medium molecular weight compounds include cholesterol, iron and vitamin B12 polypeptides, etc. 4.1.3. The macromolecular compounds include proteins and growth factors. 4.1.4. The virus is Influenza virus, Coronavirus, hepatitis virus, Hepatitis B virus, Hepatitis C virus, Human immunodeficiency virus, Varicella-zoster virus, Measles virus, Rubella virus, Adenovirus, Enterovirus, Yellow fever virus, Human papillomavirus, Human respiratory syncytial virus, Rotavirus, Adenovirus type 36, Adenovirus type 6, Adenovirus type 11, Adenovirus type 7, Adenovirus type 5, Adenovirus type 4, Adenovirus type 3, Adenovirus type 2, Adenovirus type 1, Adenovirus type 40, Adenovirus type 41, Parainfluenza virus, Japanese encephalitis virus, Human immunodeficiency virus type 2 (HIV-2), Human herpes simplex virus, Respiratory syncytial virus type 1, Respiratory syncytial virus type 2, Respiratory syncytial virus type 3, Herpes zoster virus, Lyme disease virus, Human immunodeficiency virus type 1 (HIV-1), Porcine parvovirus, Picornaviridae, Norovirus, Parainfluenza virus, Influenzavirus), Norovirus, Hepatitis A virus, Calicivirus; Viruses that animals are susceptible to: Feline infectious peritonitis virus (FIPV), feline panleukopenia virus (FPV), feline coronavirus (FCoV), feline immunodeficiency virus (FIV), feline leukemia virus (FeLV), feline calicivirus, feline viral rhinotracheitis virus (FVRV), feline infectious anemia virus (Haemobartonella felis), feline borna disease virus, feline leptospira virus (Borrelia burgdorferi), rabies virus, canine distemper virus, canine coronavirus, canine infectious hepatitis virus, canine parvovirus, canine influenza virus, canine viral diarrhea virus, canine oral papillomavirus, canine herpesvirus, canine immunodeficiency virus, foot-and-mouth disease virus, bovine respiratory syncytial virus, rinderpest virus, bovine viral diarrhea virus, ovine viral diarrhea virus, bluetongue virus, infectious bronchitis virus, Marek’s disease virus, Newcastle disease virus, duck plague virus, duck hepatitis virus, goose parvovirusparvovirus), Infectious laryngotracheitis virus, Goose hepatitis B virus, Goose astrovirus, Equine foot-and-mouth disease virus, Porcine parvovirus, Swine influenza virus, Porcine reproductive and respiratory syndrome virus, Porcine epidemic diarrhea virus, Porcine viral diarrhea virus, Porcine parainfluenza virus, Mycoplasma hyopneumoniae, Porcine encephalomyelitis virus, Porcine vesicular virus, Herpes virus, Bovine viral diarrhea virus (BVDV), Bovine papillomavirus, Contagious bovine pleuropneumonia virus, Bovine enterovirus, Bovine coronavirus, Goose plague virus, Duck infectious hepatitis virus, Duck infectious laryngotracheitis virus, Duck infectious gastroenteritis virus, Goose infectious gastroenteritis virus, Avian influenza virus, Newcastle disease virus, Infectious bronchitis virus, Inflammatory bowel disease virus, Infectious anemia virus of chicken, Infectious coryza virus, Infectious laryngotracheitis virus, Infectious hepatitis virus of chicken, Infectious diarrhea virus of chicken. 4.1.5. The pathogenic microorganism is Mycoplasma, Chlamydia, Bordetella pertussis, Candida, Actinomyces, Treponema pallidum; Escherichia coli, Staphylococcus aureus, Mycobacterium tuberculosis, Pseudomonas aeruginosa, Klebsiella pneumoniae, Salmonella, Proteus mirabilis, Bacillus, Streptococcus pneumoniae, Methicillin-resistant Staphylococcus aureus (MRSA), Vibrio cholerae, Clostridium difficile, Neisseria gonorrhoeae, Clostridium tetani, Listeria monocytogenes, Clostridium perfringens, Mycobacterium tuberculosis, Candida albicans, Aspergillus, Histoplasma, Trichophyton, Cryptococcus, Blastomyces, Pneumocystis, Clostridium, Phytophthora, Saccharomyces, Fusarium, Sporothrix, Malassezia, Coccidioides, Actinomyces, Bacillus anthracis, Rhizopus, Pneumocystis carinii, Zygomycetes, etc. 4.1.6. The nano-drugs include polymer, metal, semiconductor or ceramic nano-drugs, liposome drugs, nanotube drugs, and nucleic acid nano-drugs. 4.1.7. The nanoparticles include metal nanoparticles, quantum dots, magnetic nanoparticles, and polymer nanoparticles. 4.2. The prevention, inhibition or reduction of the invasion of viruses, bacteria, Chlamydia, Mycoplasma, and fungi into cells through membrane penetration transport methods such as cell endocytosis or membrane fusion is used for the prevention of virus, bacteria, Chlamydia, Mycoplasma, and fungal infections. 4.3. Non-specific phagocytosis of nanoparticles or nano-drugs by cells can be blocked, inhibited or reduced, thereby enabling more nano-drugs to enter the target site and improving the effective utilization of nano-drugs. 4.5. Influence of the water-soluble carbon chain on exosomes 4.5.1. The water-soluble carbon chain can increase and promote the extracellular release of exosomes of insulin from pancreatic islet cells within a certain concentration range, and can inhibit or reduce the extracellular release of exosomes of insulin from pancreatic islet cells within another concentration range. 4.5.2. The water-soluble carbon chain can increase and promote the extracellular release of exosomes of white blood cells, hepatocytes, mammary gland cells, and nerve cells within a certain concentration range, and can inhibit or reduce the extracellular release of exosomes of white blood cells, hepatocytes, mammary gland cells, and nerve cells within another concentration range.
[0256] 5. Use of a water-soluble carbon chain that increases the fluidity of the cell membrane 5.1. The water-soluble carbon chain can increase the fluidity of the membrane at a certain concentration and promote cell growth and division. 5.2. By increasing the fluidity of the cell membrane, the phospholipid bilayer within the cell membrane changes from a liquid crystal state to a liquid state, resulting in the rupture of the cell membrane and being used to destroy the cell membranes of viruses, Mycoplasma, Chlamydia, bacteria, and fungi having a lipid envelope, and is used for the treatment of virus, Mycoplasma, Chlamydia, bacteria, and fungal infections. 5.2.1. The inactivated enveloped virus includes that the enveloped virus is one or more of coronavirus, influenza virus, human immunodeficiency virus, hepatitis B virus, hepatitis C virus, herpes virus, Zika virus, dengue virus, Japanese encephalitis virus, Ebola virus, monkeypox virus, respiratory syncytial virus, and / or hantavirus. 5.2.2. The inactivated bacteria, mycoplasma, chlamydia, and fungi include that the bacteria are Gram-positive bacteria and / or Gram-negative bacteria, the fungi are pathogenic fungi and / or conditional pathogenic fungi, the chlamydia are Chlamydia trachomatis, Chlamydia pneumoniae, and / or Chlamydia psittaci, and the mycoplasma are Mycoplasma pneumoniae, Mycoplasma ureaplasma, Mycoplasma hominis, and / or Mycoplasma genitalium. 5.2.3. The bacteria are one or more selected from Escherichia coli, Staphylococcus aureus, methicillin-resistant Staphylococcus aureus, Streptococcus pneumoniae, Klebsiella pneumoniae, and Pseudomonas aeruginosa, and the fungi are one or more selected from Candida albicans, Aspergillus niger, anaerobic positive bacilli, ascomycetes, Aspergillus proteus, and Microsporum canis.
[0257] 6. Use of the water-soluble carbon chain that reduces the fluidity of the cell membrane within a certain concentration range. 6.1. The water-soluble carbon chain maintains the stability of the membrane by reducing the fluidity of the cell membrane and reduces cell division and proliferation. 6.2. The water-soluble carbon chain reduces and suppresses the release of intracellular inflammatory factors due to cell membrane rupture, thereby reducing the inflammatory reaction and degree. 6.3. The water-soluble carbon chain has the effects of preventing body aging and skin aging by affecting the fluidity of the cell membrane. 6.4. The water-soluble carbon chain neutralizes inflammatory mediators to suppress inflammation, thereby having the effects of preventing aging and skin aging.
[0258] 7. The water-soluble carbon chain can prevent, inhibit, or reduce the entry of a virus into a host cell through endocytosis or membrane fusion within a certain concentration range, and is used for preventing human or animal virus infections. 7.1. The virus includes the following. 7.1.1. Enveloped viruses and non-enveloped viruses; 7.1.2. DNA viruses and RNA viruses: double-stranded DNA viruses, single-stranded DNA viruses, double-stranded RNA viruses, sense single-stranded RNA viruses: antisense single-stranded RNA viruses, retroviruses, RNA retroviruses, DNA retroviruses; 7.2. Includes preventing infections of human viruses, animal viruses, and plant viruses. 7.3. The virus includes one or more of the following: coronavirus, influenza virus, human immunodeficiency virus, hepatitis B virus, hepatitis C virus, herpes virus, Zika virus, dengue virus, Japanese encephalitis virus, Ebola virus, hantavirus, poliovirus, adenovirus, herpes zoster virus: herpes simplex virus (HSV), varicella-zoster virus (VZV), human papillomavirus (HPV), smallpox virus (Variola virus) and monkeypox virus (Monkeypox virus) including orthopoxvirus, African swine fever virus (Asfarviridae), rotavirus, measles virus, bunyavirus, flavivirus, reovirus, sarcoma virus family, filovirus family, bullet virus family rabies virus, parainfluenza virus family, ribovirus, prion.
[0259] 8. The water-soluble carbon chain can prevent chronic diseases caused by virus infections within a certain concentration range. 8.1. It can prevent neurodegenerative diseases caused by bacterial infections, including Alzheimer's disease (AD), Parkinson's disease (PD), Huntington's disease (HD), amyotrophic lateral sclerosis (ALS), various types of spinocerebellar ataxia (SCA), and Pick's disease. 8.2. It can prevent acquired immunodeficiency syndrome (AIDS) caused by the human immunodeficiency virus (HIV). It can prevent oral herpes, genital herpes, and other skin lesions caused by herpes simplex virus (HSV) infection. It can prevent herpes zoster and postherpetic neuralgia caused by varicella-zoster virus (VZV) infection. It can prevent infections and diseases after organ transplantation, congenital infections in newborns, and lesions in immunodeficient individuals caused by human cytomegalovirus (HCMV). It can prevent adult T-cell leukemia / lymphoma (ATL) and HTLV-1-related myeloid diseases caused by human T-cell lymphotropic virus (HTLV-1) infection. It can prevent mumps, pityriasis rosea, and post-infection fatigue syndrome caused by human herpesvirus 6 (HHV-6) infection.
[0260] 9. Use of the water-soluble carbon chain that affects cell migration and locomotion. 9.1. It can promote the deformation and migration of macrophages, immune cells T lymphocytes, B lymphocytes, dendritic cells, and NK cells within a certain concentration range and is used as adjuvant therapy in immunotherapy. It suppresses the deformation and migration of macrophages, immune cells T lymphocytes, B lymphocytes, dendritic cells, and NK cells within another concentration range. 9.2. It can promote the deformation and migration of melanocytes within a certain concentration range and suppresses the deformation and migration of melanocytes within another concentration range. 9.3. It can promote the deformation and migration of hair follicle cells within a certain concentration range and suppresses the deformation and migration of hair follicle cells within another concentration range. 9.4. It can promote the deformation and migration of endothelial cells within a certain concentration range and suppresses the deformation and migration of endothelial cells within another concentration range. 9.5. It can promote the deformation and migration of epithelial cells within a certain concentration range and inhibit the deformation and migration of epithelial cells in another concentration range. 9.6. It can promote the deformation and migration of white blood cells within a certain concentration range and inhibit the deformation and migration of white blood cells in another concentration range.
[0261] 10. The water-soluble carbon chain substance can neutralize inflammatory mediators. 。 10.1. The water-soluble carbon chain substance can neutralize small molecule inflammatory mediators: neurotransmitter substances such as oxygen radicals, nitrogen radicals, prostaglandins, histamine, leukotrienes, and serotonin. 10.2. The water-soluble carbon chain can neutralize large molecule inflammatory mediators such as tumor necrosis factor (TNF), interleukins (IL-1, IL-6, IL-8, etc.), thromboxane, protease, and angiotensin, act with these large molecule inflammatory molecules, and inhibit the inflammatory reaction.
[0262] 11. The water-soluble carbon chain substance can be made into pharmaceutical preparations, cosmetics, skin care products, dietary supplements, and environmental disinfection and sterilization preparations. 11.1. The pharmaceutical preparation is one selected from inhalants, nasal sprays, injections, oral preparations, liposome emulsion dosage forms, ointments, oils, and topical skin dosage forms. 11.2. It is the use of the water-soluble carbon chain substance in the preparation of a pharmaceutical preparation for preventing, blocking, and / or treating microbial infections or an environmental disinfection and sterilization microbial reagent. 11.3 The preparation method of the water-soluble carbon chain substance is to react a compound having a lipophilic saturated and / or unsaturated carbon chain with a branched, cyclic structure, and / or linear structure, a water-soluble molecule, a protein, polypeptide, amino acid, oligopeptide, oligosaccharide, monosaccharide, and / or polysaccharide molecule that can bind to the surface of the microbial lipid membrane or cell wall, which can be added as needed, and a linker molecule that can be added as needed, in the presence of a catalyst to obtain the complex. 11.3.1. The preparation method of the water-soluble carbon chain substance is a purified product of the compound from which the water-soluble carbon chain substance is obtained by reaction. 11.4. The preparation method of the water-soluble carbon chain substance is to physically mix a compound having a lipophilic saturated and / or unsaturated carbon chain with a branched, cyclic structure and / or a linear structure, a water-soluble molecule, and optionally a protein, polypeptide, amino acid, oligopeptide, oligosaccharide, monosaccharide, and / or polysaccharide molecule that can bind to the surface of the microbial lipid membrane or the cell wall to obtain the complex. 11.5. The preparation method of the water-soluble carbon chain substance is to react a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms with any one substance of protein, polypeptide, oligopeptide, oligosaccharide, monosaccharide, disaccharide, oligonucleotide, vitamin, water-soluble polymer, water-soluble polyamino acid, and / or polysaccharide in the presence of a catalyst to obtain the complex. 11.5.1. The preparation method of the water-soluble carbon chain substance is that the complex is a purified product of the compound obtained by the reaction. 11.6. The preparation method of the water-soluble carbon chain substance is to complex a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms with a protein, polypeptide, oligopeptide, oligosaccharide, monosaccharide, disaccharide, oligonucleotide, vitamin, water-soluble polymer, water-soluble polyamino acid, and / or polysaccharide molecule by physicochemical action to obtain the complex, or directly physically mix them to obtain the complex.
[0263] Specifically, in one embodiment, the present invention provides a complex for preventing, inhibiting, or treating microbial infections. The complex of the present invention includes an active portion, a binding portion, and a water-soluble portion.
[0264] The active portion is a lipophilic hydrophobic carbon chain, which may exist in the form of a molecule or in the form of a molecular residue, and the carbon chain is a saturated and / or unsaturated carbon chain having a branched and / or linear structure, and by inserting / fusing into the lipid membrane of the microorganism, it can destroy the structure of the lipid membrane or enclose a non-enveloped virus to hydrophobically isolate the virus. The binding moiety may be a molecule or a residue of a molecule, and can bind to a microbial lipid membrane, a microbial surface protein, a microbial surface polysaccharide, or a cell wall component (including polysaccharides or proteins), or can bind to a polysaccharide, protein, or polypeptide in a microorganism, whereby the complex is linked to the microbial lipid membrane or the virus surface.
[0265] The water-soluble moiety is a molecule or a residue of a molecule that is soluble in water, contains a water-soluble group, can impart water solubility to the complex, can uniformly disperse the complex in an aqueous solution, can avoid aggregation of the lipophilic hydrophobic groups, and can avoid aggregation of the lipophilic hydrophobic groups of the complex in an aqueous solution or in blood to form lipid droplets.
[0266] More specifically, the active moiety is a saturated and / or unsaturated carbon chain having a lipophilic hydrophobic branch, cyclic structure, and / or linear shape, the carbon chain is a molecule or a residue of a molecule, and the carbon chain is a carbon chain having 3 to 100 carbon atoms. The water-soluble moiety is a molecule or a residue of a molecule that is soluble in water, and the molecule contains one or more groups selected from an amide group, a phosphoryloxy group, a carboxylic acid group, a phosphate group, a sulfonic acid group, a sulfonyloxy group, a hydroxy group, a quaternary ammonium group, a thioether group, a disulfide bond, an ether group, a mercapto group, an amine group, an amino group, a urea group, and a guanidino group. The water-soluble moiety may be a group that links to the carbon chain that is the active moiety. The binding moiety can bind to a microbial lipid membrane, a microbial surface protein, a microbial surface polysaccharide or a cell wall component, or to a polysaccharide, protein or polypeptide in a microbe, and is a molecule or a residue of a molecule. The binding moiety is the same as the water-soluble moiety, i.e., it may be a protein, polypeptide, oligopeptide, oligosaccharide, monosaccharide and / or polysaccharide molecule or a residue thereof that can bind to a microbial lipid membrane or a surface domain. The binding moiety is the same as the water-soluble moiety, i.e., after forming a complex, it retains one or more of a free carboxyl group, a phosphate group, a sulfonic acid group, a hydroxy group, a mercapto group, an amine group, an amino group, a urea group, and a guanidino group. In some cases, the binding moiety may be a divalent or polyvalent fatty acid or a lipid-soluble amino acid molecule or a residue thereof that can bind to a microbial lipid membrane or a surface domain. In this case, the carboxylic acid group and the amino acid group in these divalent or polyvalent fatty acids or lipid-soluble amino acid molecules or residues substantially perform a binding function.
[0267] Specifically, here the active moiety is a lipid-soluble carbon chain, including a saturated or unsaturated carbon chain with a branched and cyclic structure. Preferably, the active moiety is a carbon chain or a carbon chain residue having 3 to 48 carbon atoms, more preferably 3 to 26 carbon atoms, formed by a substance selected from saturated and / or unsaturated aliphatic hydrocarbons, saturated and / or unsaturated aliphatic alcohols or oxoaliphatic alcohols, saturated and / or unsaturated fatty acids, hydrophobic amino acids, lipid-soluble vitamins, steroid lipids, phospholipids, sphingomyelin, glycolipids, and surfactants. Here, preferably, the number of carbon atoms is 3 to 26. The water-soluble moiety is a water-soluble molecule or a residue of a molecule containing one or more groups selected from a mercapto group, an amino group, a phosphate group, a carboxylic acid group, a sulfonic acid group, a hydroxy group, an amine group, a urea group, a guanidino group, and a disulfide group, and the group that exerts the binding action of the binding moiety (which can bind to a microbial lipid membrane, a microbial surface protein, a microbial surface polysaccharide, or a cell wall component, or can bind to a polysaccharide, protein, or polypeptide in a microorganism) is a group selected from a mercapto group, an amino group, a phosphate group, a carboxylic acid group, a sulfonic acid group, a hydroxy group, an amine group, a urea group, a guanidino group, and a disulfide group derived from the water-soluble moiety, or a group selected from a mercapto group, an amino group, a phosphate group, a carboxylic acid group, a sulfonic acid group, a hydroxy group, an amine group, a urea group, a guanidino group, and a disulfide group that provides a linkage between carbon chains.
[0268] Specifically, for the complex of the present invention, the water-soluble moiety is a water-soluble molecule or a residue of a molecule, including macromolecular proteins, polysaccharides, nucleic acids, artificially synthesized water-soluble polymers, medium-sized polypeptides, oligopeptides, oligosaccharides, oligonucleotides, and artificially synthesized water-soluble medium polymers. Small molecules include amino acids, monosaccharides or disaccharides, nucleotides, and water-soluble vitamins. Functional groups that can increase water solubility by directly binding to a carbon chain, such as an amide group, a phosphoryloxy group, a carboxylic acid group, a phosphate group, a sulfonic acid group, a sulfonyloxy group, a hydroxy group, a quaternary ammonium group, a thioether group, a disulfide bond, an ether group, a mercapto group, an aldehyde group, an ester group, an amine group, an amino group, a urea group, a guanidino group, etc. may also be used. The water-soluble moiety may be a group that links to the carbon chain of the functional moiety and / or the binding moiety. The binding moiety is a molecule or a residue of a molecule (including functional groups on the molecule) that can bind to a microbial lipid membrane, a microbial surface protein, a microbial surface polysaccharide, or a cell wall component, and may be the third part constituting the complex, may be the same as the water-soluble part, or may be linked to the active part. When the binding moiety is the same part as the water-soluble part, for example, a protein, polypeptide, polysaccharide, etc. that can bind to a microbial lipid membrane, a microbial surface protein, or a microbial surface polysaccharide, the water-soluble part contains one selected from a mercapto group, an amino group, a urea group, a guanidino group, a carboxylic acid group, a hydroxy group, and a disulfide group. The binding moiety may, in some cases, be a divalent fatty acid or a polyvalent fatty acid, a lipophilic amino acid, etc. that binds to a microbial lipid membrane, a microbial surface protein, or a microbial surface polysaccharide.
[0269] Although not limited to the reaction mechanism, the functional group that exerts the binding action of the binding moiety may be a carboxyl group, a sulfonic acid group, a phosphate group, a hydroxy group, an aldehyde group, or a hydroxy group of a hemiacetal (saccharide), an amino group, a urea group, a guanidino group, a mercapto group, etc.
[0270] 1. Hereinafter, an example in which a fatty acid is a carbon chain donor (i.e., an active part donor) will be further described. (1) Fatty acids are insoluble in water or have extremely low water solubility and cannot be directly injected into the body. If directly injected intravenously, it will cause pulmonary embolism, and if injected into an artery, it will cause arterial embolism and tissue necrosis. (2) Fatty acids are re-esterified within enterocytes, mixed with bile salts and monoglycerides to form fat particles of 4 to 6 nm, and these fat particles are directly absorbed by enterocytes through phagocytosis, coated on the outside with a membrane of lecithin and protein, becoming chylomicrons, entering the lymphatic system, passing through lymphatic vessels and the thoracic duct, and returning to the bloodstream in the form of an oil-in-water emulsion. Medium-chain fatty acids, except for a small amount that exists in peripheral blood for a short period, are mostly non-covalently bound to serum proteins and rapidly reach the liver through the portal system. In the liver, medium-chain fatty acids quickly pass through the mitochondrial double membrane and are rapidly acylated by the action of octanoyl CoA, but are hardly synthesized into fat. The excess acetyl CoA generated by acylation undergoes various metabolic effects in the cytoplasm of mitochondria, and most of it tends to synthesize ketone bodies. (3) Fatty acids covalently bound to large, medium, and small molecules change lipophilic fatty acids into water-soluble fatty acids, and moreover, they are not easily removed from the liver and metabolized. (4) The highly water-soluble and highly affinity complex of the present invention has an anti-microbial infection effect and can be used not only in topical skin dosage forms, but also in nasal sprays, dry powder inhalants, and even intravenous injections and oral dosage forms.
[0271] 2. Complex formed by fatty acids and water-soluble amino acids, monosaccharides or disaccharides, nucleotides, water-soluble vitamins At this time, the carbon chain of the fatty acid is the acting part, and the water-soluble amino acid, monosaccharide or disaccharide, nucleotide, water-soluble vitamin is the water-soluble part. When linked to the binding part, it constitutes a complex having the anti-microbial infection effect described in the present invention. The binding part may be selected from divalent fatty acids or polyvalent fatty acids, amino acids, targeting proteins, targeting polypeptides, targeting polysaccharides. Here, divalent fatty acids or polyvalent fatty acids and lipophilic amino acids are both the acting part and the binding part, and water-soluble amino acids, targeting proteins, targeting polypeptides, targeting polysaccharides are both the water-soluble part and the binding part. 。
[0272] In a specific embodiment, the complex of the present invention is selected from complexes formed by linking a fatty trienoic acid having 3 to 50 carbon atoms and a water-soluble amino acid. For example, the following compound may be a complex formed by linking octadecatrienoic acid to aspartame.
Chemical formula
[0273] 3. Complexes formed by fatty acids and proteins, polypeptides, and polysaccharides At this time, the carbon chain of the fatty acid is the active part, and the protein or polypeptide targeting the virus surface domain, lipid membrane, or cell wall, and the polysaccharide are both the binding part and the water-soluble part. In a specific embodiment, the complex of the present invention is selected from complexes formed by linking an aliphatic alkene acid having 3 to 50 carbon atoms to a targeting polypeptide. For example, the following structural formula may be a schematic structural formula of a complex formed by linking octadecenoic acid to a targeting polypeptide, in which the octadecenoic acid and the lysine residue in the polypeptide are linked by an amide bond.
Chemical formula
[0274] Here, the carbon chain of octadecenoic acid is the active part, and the targeting polypeptide is both the water-soluble part and the binding part.
[0275] 4. When the water solubility of the complex is low in the above three cases, or when it is necessary to increase the size of the complex molecule, a water-soluble polymer can be added. For example, fatty acid + targeting polypeptide + PEG, that is, the complex is a complex formed by reacting a fatty acid having 3 to 50 carbon atoms, a targeting polypeptide, and PEG. At this time, the carbon chain of the fatty acid is the active part, the targeting polypeptide is the binding part, and PEG is the water-soluble part.
[0276] 5. Compounds such as fatty alcohol polyoxyethylene ether, fatty acid polyoxyethylene ester, alkyl polyglucoside, sucrose fatty acid ester, sorbitan fatty acid ester, polyoxyethylene sorbitan fatty acid ester, mannosyl erythritol lipid, N-fatty acyl-N-methylglucosamine have an aliphatic alcohol or fatty acid as a carbon chain donor and have good water solubility, but have a weak binding effect with virus surface domains, lipid membranes or cell wall components, and a relatively high concentration is required to kill microorganisms. At this concentration, these compounds also have a destructive effect on human cells and are not suitable for internal use in the human body. When the above compounds are linked to the binding part to form a new complex, microorganisms can be killed at a relatively low concentration in the human body, achieving the effect of anti-microbial infection. Also, at this therapeutic concentration, the new complex having the active part + water-soluble part + binding part does not affect human tissue cells and organs. The binding part may be selected from dibasic fatty acids or polybasic fatty acids, amino acids, targeting proteins, targeting polypeptides, and targeting polysaccharides. That is, in this case, the complex of the present invention is a complex formed by reacting a surfactant with one or more selected from dibasic fatty acids or polybasic fatty acids, amino acids, targeting proteins, targeting polypeptides, and targeting polysaccharides. At this time, the carbon chain of the aliphatic alcohol or fatty acid is the active part, polyoxyethylene ether (PEG), glucan, sucrose, sorbitan, mannoerythritol, glucosamine are the water-soluble parts, and the linked dibasic fatty acid or polybasic fatty acid and lipophilic amino acid are both the binding part and the active part, while water-soluble amino acids, targeting proteins, targeting polypeptides, and targeting polysaccharides are both the binding part and the water-soluble part.
[0277] Specifically, in a specific embodiment of the present invention, the present invention provides a complex capable of preventing and treating viral, bacterial, and fungal infections, and its main structure is formed by a functional part, a binding part, and a water-soluble part through covalent bonds, hydrogen bonds, or van der Waals force coupling. The functional part gives the complex the function of destroying the microbial lipid membrane or hydrophobically isolating non-enveloped viruses. The binding part gives the complex the function of binding to the microbial lipid membrane or viral surface domain. A specific binding part also gives the complex the function of specifically targeting microorganisms. The water-soluble part gives the complex water solubility, uniformly disperses the complex in an aqueous solution, and avoids the aggregation of hydrophobic groups to form lipid droplets.
[0278] The lipid membrane is the envelope formed by the phospholipid bilayer of microorganisms. The functional part, binding part, and water-soluble part in the complex may be natural compounds, artificially synthesized compounds, or compounds in which natural compounds are coupled to artificially synthesized compounds. The number of groups of the same kind in the complex may be one or more, and the arrangement method and order of each group are not fixed. The same kind or different kinds of groups may be linearly coupled or coupled through side chains.
[0279] The complex is used for the prevention and treatment of infectious diseases caused by viruses, bacteria, fungi, Chlamydia, and Mycoplasma.
[0280] Furthermore, the functional part is a natural or artificially synthesized hydrophobic group, including a linear carbon chain, a branched carbon chain, and a carbon chain with a cyclic structure. The carbon chain may be a saturated / unsaturated carbon chain, and the unsaturated carbon chain may have one or more unsaturated bonds, where the unsaturated bond may be a double bond or a triple bond. For microorganisms having a lipid membrane structure, such as enveloped viruses, bacteria, fungi, Chlamydia, and Mycoplasma, the active moiety can penetrate, insert into, and fuse with the lipid membrane, disrupt the structural stability of the lipid membrane, and further disrupt the integrity of the lipid membrane and cell wall, achieving the effect of killing the microorganism. In the case of non-enveloped viruses, the binding moiety binds to the viral surface protein domain, and the active moiety is encapsulated on the surface of the non-enveloped virus, hydrophobically isolating the non-enveloped virus and being removed by immune cells, achieving the effect of preventing and treating non-enveloped virus infection.
[0281] Furthermore, the binding moiety has one or more functional groups capable of binding to proteins, polysaccharides, or bindable domains, such as carboxyl groups, hydroxyl groups, amino groups, mercapto groups, urea groups, guanidino groups, and can bind to proteins, polysaccharides, or bindable domains on the lipid membrane or viral surface, and the complex is linked to the lipid membrane or viral surface. The binding moiety may further be designed to have a molecular structure that specifically targets the lipid membrane, cell wall components of bacteria and fun...
Claims
1. It includes an active part, a binding part, and a water-soluble part. Here, the virus is one or more viruses selected from the group consisting of novel coronavirus, influenza virus, human immunodeficiency virus, hepatitis B virus, human herpes virus, Ebola virus, rabies virus, and human papillomavirus, and the bacterium is one or more bacteria selected from the group consisting of Escherichia coli, Staphylococcus aureus, methicillin-resistant Staphylococcus aureus, Streptococcus pneumoniae, Klebsiella pneumoniae, and Pseudomonas aeruginosa. The active part is a lipophilic saturated and / or unsaturated carbon chain having a branched, cyclic structure and / or a linear structure. The carbon chain is a molecule or a residue of a molecule. The carbon chain is a carbon chain having 3 to 100 carbon atoms. Here, the active part is a carbon chain having 3 to 100 carbon atoms or a residue of a carbon chain formed by saturated and / or unsaturated fatty acids. The water-soluble part is a molecule or a residue of a molecule that is soluble in water. The molecule contains one or more functional groups selected from the group consisting of an amide group, a phosphoryloxy group, a carboxylic acid group, a phosphate group, a sulfonic acid group, a sulfonyloxy group, a hydroxy group, a quaternary ammonium group, a thioether group, a disulfide bond, an ether group, a mercapto group, an aldehyde group, an ester group, an amine group, an amino group, a urea group, and a guanidino group. The water-soluble part is one or more of the above functional groups linked to the carbon chain that is the active part. The binding part is a molecule or a residue of a molecule that can bind to a microbial lipid membrane, a microbial surface protein, a microbial surface polysaccharide, or a cell wall component, or can bind to a polysaccharide, protein, or polypeptide in a microorganism. The binding part is the same as the water-soluble part, that is, a protein, polypeptide, amino acid, oligopeptide, oligosaccharide, monosaccharide, and / or polysaccharide molecule or its residue that can bind to a microbial lipid membrane or a surface domain. Here, the number of any one of the active part, the water-soluble part, and the binding part is one or more, and it is a complex capable of preventing, inhibiting, and / or treating virus or bacterial infection.
2. The complex according to Claim 1, wherein the number of carbon atoms is 3 to 48.
3. The complex according to Claim 1, wherein the number of carbon atoms is 3 to 26.
4. The water-soluble portion is a water-soluble molecule or a residue of a molecule containing one or more groups selected from a mercapto group, an amino group, a phosphate group, a carboxylic acid group, a sulfonic acid group, a hydroxy group, an amine group, a urea group, a guanidino group, and a disulfide group. The binding portion has a group that exerts a binding action, that is, it can bind to a microbial lipid membrane, a microbial surface protein, a microbial surface polysaccharide, or a cell wall component, or can bind to a polysaccharide, protein, or polypeptide in a microorganism. This group is derived from the water-soluble portion or independently from two or more groups selected from a mercapto group, an amino group, a phosphate group, a carboxylic acid group, a sulfonic acid group, a hydroxy group, an amine group, a urea group, a guanidino group, and a disulfide group that form the binding portion, or is derived from one or more groups selected from a mercapto group, an amino group, a phosphate group, a carboxylic acid group, a sulfonic acid group, a hydroxy group, an amine group, a urea group, a guanidino group, and a disulfide group that provide a linkage between carbon chains. Thereby, the complex has one or more groups among a mercapto group, an amino group, a phosphate group, a carboxylic acid group, a sulfonic acid group, a hydroxy group, an amine group, a urea group, a guanidino group, and a disulfide group. The complex according to claim 1.
5. The complex according to claim 4, wherein the binding portion is one or more selected from a divalent fatty acid or a polyvalent fatty acid, an amino acid, a targeting protein, a targeting polypeptide, and a targeting polysaccharide.
6. The complex is a complex formed by linking a fatty acid having 3 to 50 carbon atoms with a water-soluble amino acid, or the complex is a complex formed by linking a fatty acid having 3 to 50 carbon atoms to a targeting polypeptide, or the complex is a complex formed by reacting a fatty acid having 3 to 50 carbon atoms, a targeting polypeptide, and PEG, or the complex is a complex formed by reacting a surfactant with one or more selected from a divalent fatty acid or a polyvalent fatty acid, an amino acid, a targeting protein, a targeting polypeptide, and a targeting polysaccharide. The complex according to claim 4.
7. The saturated and / or unsaturated fatty acid is selected from saturated or unsaturated fatty acids having 3 to 50 carbon atoms, and the fatty acid contains a double bond, a triple bond, a hydroxy group, an amino group, and / or is a fatty acid or amino acid substituted with oxygen, and is a monobasic acid, a dibasic acid or a polybasic acid. The complex according to claim 4.
8. The saturated and / or unsaturated fatty acid is a saturated fatty acid having 3 to 46 carbon atoms, a monoenoic acid having 3 to 34 carbon atoms, a dienoic acid having 5 to 30 carbon atoms, a trienoic acid having 7 to 30 carbon atoms, a tetraenoic acid having 12 to 38 carbon atoms, a pentaenoic acid having 12 to 38 carbon atoms, a hexaenoic acid having 22 to 38 carbon atoms, an acetylenic acid having 6 to 22 carbon atoms, a diacetylenic acid having 10 to 22 carbon atoms, a triacetylenic acid having 12 to 22 carbon atoms, an enynoic acid having 8 to 20 carbon atoms, a fatty acid having an alkyl group with a main chain carbon number of 3 to 30 and a branched carbon number of 1 to 10 and / or 1 to 3 hydroxy groups, a saturated linear and branched dicarboxylic acid and tricarboxylic acid having 3 to 38 carbon atoms, an unsaturated linear or branched dicarboxylic acid and tricarboxylic acid having 4 to 18 carbon atoms which may be substituted with a hydroxy group, a carboxylic acid substituted with an amino group, a hydroxy group, an oxo group and / or a methyl group having 3 to 18 carbon atoms, an N-fatty acyl amino acid having 6 to 30 carbon atoms, an amino acid containing two or more fatty acyls, and a polycarboxylic acid linked by a thioether bond and an amide bond, and is one or more selected therefrom. The complex according to claim 4.
9. The saturated and / or unsaturated fatty acid is one or more selected from fumaric acid, caprylic acid, glutaconic acid, hexanoic acid, nonanoic acid, dodecanoic acid, tetradecanoic acid, hexadecanoic acid, octadecanoic acid, eicosanoic acid, oleic acid, linoleic acid, linolenic acid, eicosapentaenoic acid, docosapentaenoic acid, docosahexaenoic acid, pentacosanoic acid, enanthic acid, decanoic acid, dodecenoic acid, tetradecenoic acid, dotriacontanehexaenoic acid, octacosanoic acid, or a carbon chain residue formed by these. The complex according to claim 4.
10. The water-soluble portion is a molecule or a residue of a molecule containing one or more groups selected from a mercapto group, an amino group, a carboxylic acid group, a hydroxy group, and a disulfide group, and the molecule is one or more water-soluble macromolecules or residues thereof selected from proteins, polysaccharides, nucleic acids, and artificially synthesized water-soluble polymers, and / or one or more medium molecules or residues thereof selected from polypeptides, oligopeptides, oligosaccharides, oligonucleotides, and artificially synthesized medium molecular weight water-soluble polymers, and / or one or more water-soluble small molecules or residues thereof selected from amino acids, monosaccharides, disaccharides, nucleotides, water-soluble vitamins, and deoxyribonucleotides, and / or a molecule or a residue of a molecule linked to the carbon chain which is the active portion, and the molecule or the residue of the molecule contains one or more groups selected from a mercapto group, an amino group, a carboxylic acid group, a hydroxy group, and a disulfide group, the conjugate according to claim 4.
11. The protein which is the water-soluble macromolecule is one or more water-soluble macromolecules selected from serum albumin, immunoglobulins, water-soluble collagen, chaperones, water-soluble glycoproteins, and CD14, and the polysaccharide which is the macromolecule is one or more water-soluble macromolecules selected from glucan, hyaluronic acid, sialic acid, heparan sulfate, heparin sulfate, chondroitin sulfate, dermatan sulfate, keratan sulfate, acetylated water-soluble cellulose derivatives, β-cyclodextrin and its derivatives, and water-soluble chitosan derivatives, and the water-soluble polymer which is the macromolecule is one or more water-soluble macromolecules selected from polyethylene glycol and carboxylated or aminated polyethylene glycol, polyvinyl alcohol and carboxylated or quaternized polyvinyl alcohol, polyacrylic acid, and ammonium polyacrylate, The medium molecular weight water-soluble polymer is one or more substances selected from targeting polypeptides, oligopeptides, oligosaccharides, oligonucleotides and / or water-soluble polyamino acids, The water-soluble small molecule monosaccharide and / or disaccharide is one or more selected from glucose, fructose, rhamnose, sorbose, sucrose, maltose, lactose, and trehalose. The water-soluble small molecule nucleotide and / or deoxyribonucleotide is selected from adenylate, guanylate, uridylate, cytidylate, thymidylate, inosine, deoxyadenylate, deoxyguanylate, deoxycytidylate, and deoxythymidylate. The water-soluble small molecule amino acid is one or more selected from serine, threonine, cysteine, asparagine, glutamine, tyrosine, lysine, arginine, histidine, aspartic acid, glutamic acid, citrulline, ornithine, taurine, and aminobutyric acid. The water-soluble small molecule vitamin is one or more selected from vitamin B1, pantothenic acid, vitamin B6, and vitamin C. The conjugate according to claim 10.
12. The targeting polypeptide contains any one of a specific targeting microbial lipid membrane, the cell walls of bacteria and fungi, a protein of a viral surface protein domain, or a neutralizing antibody fragment. The conjugate according to claim 11.
13. The water-soluble polyamino acid is selected from polyglutamic acid, polylysine, and / or polyaspartic acid. The conjugate according to claim 11.
14. The binding moiety is the same as the water-soluble moiety, that is, a microbial lipid membrane, a protein, polypeptide, oligopeptide, oligosaccharide, monosaccharide, disaccharide, amino acid, nucleotide, vitamin, water-soluble polymer, water-soluble polyamino acid, and / or polysaccharide molecule or a residue of these molecules that can bind to the surface domain. The molecule or the residue of the molecule contains one or more groups selected from a mercapto group, an amino group, a carboxylic acid group, a hydroxy group, and a disulfide group. The conjugate according to claim 1.
15. A compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms with at least one selected from proteins, polypeptides, oligopeptides, oligosaccharides, monosaccharides, disaccharides, nucleotides, vitamins, amino acids, water-soluble polymers, water-soluble polyamino acids, and polysaccharide molecules, or a compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 50 carbon atoms with at least one selected from proteins, polypeptides, oligopeptides, oligosaccharides, monosaccharides, disaccharides, nucleotides, vitamins, amino acids, water-soluble polymers, water-soluble polyamino acids, and polysaccharide molecules, and a mixture of the unreacted fatty acid and / or the unreacted protein, polypeptide, oligopeptide, oligosaccharide, monosaccharide, disaccharide, nucleotide, vitamin, amino acid, water-soluble polymer, water-soluble polyamino acid, and / or polysaccharide molecule, the complex according to claim 1.
16. A complex obtained by complexing a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms with at least one selected from proteins, polypeptides, oligopeptides, oligosaccharides, monosaccharides, disaccharides, nucleotides, vitamins, amino acids, water-soluble polymers, water-soluble polyamino acids, and polysaccharide molecules by physicochemical action, or a mixture directly physically mixed, wherein the physicochemical action includes hydrogen bonding or van der Waals force or a combination of both of these actions, the complex according to claim 1.
17. A compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms with at least one selected from proteins, polypeptides, oligopeptides, and amino acids, or a compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms with at least one selected from proteins, polypeptides, oligopeptides, and amino acids, and a mixture of the unreacted fatty acid and / or at least one selected from the unreacted protein, polypeptide, oligopeptide, and amino acid, the complex according to claim 15.
18. A compound obtained by reacting at least one selected from saturated and / or unsaturated fatty acids having 3 to 100 carbon atoms, PEG, and proteins, polypeptides, oligopeptides, and amino acids, or a mixture of a compound obtained by reacting at least one selected from saturated and / or unsaturated fatty acids having 3 to 100 carbon atoms, PEG, and proteins, polypeptides, oligopeptides, and amino acids with at least one selected from unreacted fatty acids, unreacted PEG, and / or unreacted proteins, polypeptides, oligopeptides, and amino acids. The complex according to claim 15.
19. A compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms with at least one selected from polysaccharides, monosaccharides, disaccharides, and oligosaccharides, or a mixture of a compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms with at least one selected from polysaccharides, monosaccharides, disaccharides, and oligosaccharides and unreacted fatty acids and / or unreacted polysaccharides, monosaccharides, disaccharides, and / or oligosaccharides. The complex according to claim 15.
20. A compound obtained by reacting at least one selected from saturated and / or unsaturated fatty acids having 3 to 100 carbon atoms, PEG, and polysaccharides, monosaccharides, disaccharides, and oligosaccharides, or a mixture of a compound obtained by reacting at least one selected from saturated and / or unsaturated fatty acids having 3 to 100 carbon atoms, PEG, and polysaccharides, monosaccharides, disaccharides, and oligosaccharides with unreacted fatty acids, unreacted PEG, and / or unreacted polysaccharides, monosaccharides, disaccharides, and / or oligosaccharides. The complex according to claim 15.
21. The protein according to claim 15 is one or more selected from serum albumin, immunoglobulins, water-soluble collagen, chaperones, water-soluble glycoproteins, and CD14.
22. The polysaccharide according to claim 15 is one or more selected from glucan and / or hyaluronic acid, sialic acid, heparan sulfate, heparin sulfate, chondroitin sulfate, dermatan sulfate, keratan sulfate, acetylated water-soluble cellulose derivatives, β-cyclodextrin and its derivatives, and water-soluble chitosan derivatives.
23. A compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms, a linker, and a protein containing a mercapto group, or a mixture of a compound obtained by the above reaction, an unreacted fatty acid, an unreacted linker, and / or a protein containing an unreacted mercapto group, wherein the linker is one or more of an amino acid, succinic acid, butadienoic acid, glutaconic acid, hexamiminodiacid, urethane, a short peptide, N-hydroxybutenimide, polyethylene glycol, and derivatives of the above compounds, the complex according to claim 15.
24. A compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms, N-hydroxybutenimide, and a protein containing a mercapto group, or a mixture of a compound obtained by the above reaction, an unreacted fatty acid, an unreacted N-hydroxybutenimide and / or a protein containing an unreacted mercapto group, the complex according to claim 23.
25. A compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms, cystamine, and at least one selected from polysaccharides, monosaccharides, disaccharides, and oligosaccharides, or a mixture of a compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 50 carbon atoms, cystamine, and at least one selected from polysaccharides, monosaccharides, disaccharides, and oligosaccharides with an unreacted fatty acid, an unreacted polysaccharide, monosaccharide, disaccharide, and at least one selected from oligosaccharides and / or an unreacted cystamine, the complex according to claim 15.
26. The compound obtained by the reaction contains one or more of an amide group, an ester group, a thioether group, or an ether group, and these groups function as a part connecting a water-soluble part and an active part, the complex according to any one of claims 15 to 25.
27. The saturated and / or unsaturated fatty acid has 3 to 50 carbon atoms, the complex according to any one of claims 4 to 25.
28. The number of carbon atoms is 3 to 48, the complex according to claim 27.
29. The number of carbon atoms is 3 to 26, the complex according to claim 27.
30. The saturated and / or unsaturated fatty acid is a fatty acid having 1 to 8 C═C double bonds and 3 to 40 carbon atoms, a fatty acid having 1 to 7 C═C double bonds, a fatty acid having 1 to 6 double bonds, a fatty acid having 1 to 5 double bonds, a fatty acid having 1 to 4 double bonds, a fatty acid having 1 to 3 double bonds, or a fatty acid having 1 to 2 double bonds. The complex according to any one of claims 4 to 25.
31. The saturated and / or unsaturated fatty acid is a fatty acid having 1 to 6 double bonds and 3 to 30 carbon atoms. The complex according to any one of claims 4 to 25.
32. The saturated and / or unsaturated fatty acid has 3 to 30 carbon atoms. The complex according to any one of claims 4 to 25.
33. The saturated and / or unsaturated fatty acid is one or more fatty acids selected from fumaric acid, caprylic acid, glutaconic acid, hexanoic acid, nonanoic acid, dodecanoic acid, tetradecanoic acid, hexadecanoic acid, octadecanoic acid, eicosanoic acid, oleic acid, linoleic acid, linolenic acid, eicosapentaenoic acid, docosapentaenoic acid, docosahexaenoic acid, pentacosanoic acid, enanthic acid, decanoic acid, dodecenoic acid, tetradecenoic acid, dotriacontanehexaenoic acid, and octacosanoic acid. The complex according to any one of claims 4 to 25.
34. The protein is human serum protein, or bovine serum protein, or CD14, or the polysaccharide is glucan and / or hyaluronic acid. The complex according to any one of claims 4 to 25.
35. The compound obtained by the reaction is a compound obtained by reacting a fatty acid with albumin or SBP1 and has one or more of the following structural formulas. The complex according to claim 17. 【Chemical 1】 [Chemical 2] 【Chemical Formula 3】 【Chemical 4】 n is an integer of 1 to 200. The complex according to claim 19.
36. The compound obtained by the reaction is one or more compounds having the following structural formula obtained by reacting a fatty acid with glucan. The complex according to claim 19. [Chemical Formula 5] 【Chemical Formula 6】 【Chemical Formula 7】 【Chemical 8】
37. The compound obtained by the reaction is one or more compounds having the following structural formula obtained by reacting a fatty acid with hyaluronic acid, 【Chemical Formula 9】 【Chemical 10】 【Chemical Formula 11】 【Chemical Formula 12】 n is an integer of 1 to 2000. The complex according to claim 19.
38. The complex according to claim 20, wherein the compound obtained by the reaction is a compound obtained by reacting a fatty acid having 3 to 10 carbon atoms, PEG, and glucose.
39. The compound obtained by the reaction is a compound having the following structural formula, The complex according to claim 38, wherein n is an integer of 1 to 200.
40. The complex according to claim 23, wherein the compound obtained by the reaction is any one or more compounds having a thioether bond and having the following structural formula, which are obtained by reacting a fatty acid, N-hydroxybutenimide, and albumin. 【Chemical 13】 【Chemical Formula 14】 【Chemical Formula 15】 【Chemical 16】
41. The complex according to claim 25, wherein the compound obtained by the reaction is any one or more compounds having the following structural formula, which are obtained by reacting a fatty acid, cystamine, and glucan. 【Chemical 17】 【Chemical Formula 18】
42. A preparation for preventing, inhibiting or treating microbial infection, prepared using the complex according to any one of claims 1 to 41.
43. The preparation according to claim 42, which is a pharmaceutical preparation or an environmental disinfection preparation.
44. The preparation according to claim 43, wherein the pharmaceutical preparation is one selected from an inhalant, a nasal spray, an injection, an oral preparation, and a topical skin preparation.
45. Use of the complex according to any one of claims 1 to 41 in the preparation of a pharmaceutical preparation or an environmental disinfection microbial reagent for preventing, inhibiting and / or treating microbial infection.
46. The use according to claim 45, wherein the microorganism is any one or two selected from viruses and bacteria.
47. The use according to claim 46, wherein the virus is an enveloped virus and / or a non-enveloped virus.
48. The use according to claim 46, wherein the virus is one or more viruses selected from novel coronavirus, influenza virus, human immunodeficiency virus (HIV), hepatitis B virus, human herpes virus, Ebola virus, rabies virus, and human papillomavirus (HPV), and the bacterium is one or more bacteria selected from Escherichia coli, Staphylococcus aureus, methicillin-resistant Staphylococcus aureus, Streptococcus pneumoniae, Klebsiella pneumoniae, and Pseudomonas aeruginosa.
49. The use according to claim 46, wherein the virus is one or more selected from H7N9 influenza virus, H5N1 influenza virus, HIV virus, novel coronavirus, HPV virus, and rabies virus.
50. A method for preparing the complex according to any one of claims 1 to 41, comprising reacting a fatty acid having a branched, cyclic structure and / or a linear structure with a lipophilic saturated and / or unsaturated carbon chain, a water-soluble molecule, a protein, polypeptide, amino acid, oligopeptide, oligosaccharide, monosaccharide and / or polysaccharide molecule that can bind to a microbial lipid membrane, microbial surface domain or cell wall, which are added as necessary, and a linker molecule that is added as necessary, in the presence of a catalyst to obtain the complex.
51. The method for preparing the complex according to claim 50, wherein the complex is a product obtained by purifying a compound obtained by the reaction.
52. A method for preparing the complex according to any one of claims 1 to 41, comprising physically mixing a fatty acid having a branched, cyclic structure and / or a linear structure with a lipophilic saturated and / or unsaturated carbon chain, a water-soluble molecule, and a protein, polypeptide, amino acid, oligopeptide, oligosaccharide, monosaccharide and / or polysaccharide molecule that can bind to a microbial lipid membrane, virus surface domain or cell wall, which are added as necessary, to obtain the complex.
53. A method for preparing the complex according to any one of claims 1 to 41, comprising reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms with any one substance selected from proteins, polypeptides, oligopeptides, oligosaccharides, monosaccharides, disaccharides, nucleotides, vitamins, amino acids, water-soluble polymers, water-soluble polyamino acids and / or polysaccharides in the presence of a catalyst to obtain the complex.
54. The method for preparing the complex according to claim 53, wherein the complex is a product obtained by purifying a compound obtained by the reaction.
55. A method for preparing the complex according to any one of claims 1 to 41, comprising complexing a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms with a protein, polypeptide, oligopeptide, oligosaccharide, monosaccharide, disaccharide, nucleotide, vitamin, amino acid, water-soluble polymer, water-soluble polyamino acid and / or polysaccharide molecule by physicochemical action to obtain the complex, or directly physically mixing them to obtain the complex.
56. A water-soluble carbon chain substance that regulates transmembrane transport and / or fluidity of cell membranes, comprising an active moiety, a binding moiety, and a water-soluble moiety, wherein the active moiety is a lipophilic saturated and / or unsaturated carbon chain having a branched, cyclic structure and / or a linear structure, the carbon chain being a molecule or a residue of a molecule, the carbon chain being a carbon chain having 3 to 100 carbon atoms, wherein the active moiety is a saturated and / or unsaturated fatty acid, aliphatic hydrocarbon or cyclic hydrocarbon, or aromatic compound or heterocyclic compound, or a salt, alcohol, ether, ester or other derivative thereof, and is a carbon chain having 3 to 100 carbon atoms or a residue of a carbon chain formed by any one or more of these, the water-soluble moiety is a molecule or a residue of a molecule soluble in water, the molecule containing one or more functional groups selected from an amide group, a phosphoryloxy group, a carboxylic acid group, a phosphate group, a sulfonic acid group, a sulfonyloxy group, a hydroxy group, a quaternary ammonium group, a thioether group, a disulfide bond, an ether group, a mercapto group, an aldehyde group, an ester group, an amine group, an amino group, a urea group, a guanidino group, and the water-soluble moiety is the above one or more functional groups linked to the carbon chain that is the active moiety, the binding moiety is a molecule or a residue of a molecule that can bind to a microbial lipid membrane, a microbial surface protein, a microbial surface polysaccharide or a cell wall component, or can bind to a polysaccharide, protein or polypeptide in the body of a microorganism, plant, animal or human, or a molecule or a residue of a molecule that can bind to a cell membrane or a surface polysaccharide or a cell wall component of a cell membrane of a plant, animal or human tissue, the binding moiety being the same as the water-soluble moiety, i.e., a protein, polypeptide, amino acid, oligopeptide, oligosaccharide, monosaccharide, disaccharide, amino acid, nucleotide, vitamin, water-soluble polymer, water-soluble polyamino acid and / or polysaccharide molecule or its residue that can bind to a microbial lipid membrane or to a surface domain of a cell membrane of a plant, animal or human tissue, wherein any one of the active moiety, the water-soluble moiety, and the binding moiety is one or more, a water-soluble carbon chain substance.
57. The water-soluble carbon chain substance according to claim 56, wherein the number of carbon atoms is 3 to 50, preferably 3 to 48, more preferably 3 to 26.
58. The water-soluble portion is a water-soluble molecule or residue of a molecule containing one or more groups selected from a mercapto group, an amino group, a phosphate group, a carboxylic acid group, a sulfonic acid group, a hydroxy group, an amine group, a urea group, a guanidino group, and a disulfide group. The binding portion has a group that exerts a binding action, that is, a molecule or residue of a molecule that binds to a microbial lipid membrane, a microbial surface protein, a microbial surface polysaccharide, or a cell wall component, or can bind to a polysaccharide, protein, or polypeptide in the body of a microorganism, plant, animal, or human, or a molecule or residue of a molecule that can bind to a cell membrane, a surface polysaccharide of a cell membrane, or a cell wall component of a tissue of a plant, animal, or human. This group is derived from the water-soluble portion or independently derived from one or more groups selected from a mercapto group, an amino group, a phosphate group, a carboxylic acid group, a sulfonic acid group, a hydroxy group, an amine group, a urea group, a guanidino group, and a disulfide group that form the binding portion, or is derived from one or more groups selected from a mercapto group, an amino group, a phosphate group, a carboxylic acid group, a sulfonic acid group, a hydroxy group, an amine group, a urea group, a guanidino group, and a disulfide group that provide a linkage between carbon chains. Thereby, the complex has one or more groups selected from a mercapto group, an amino group, a phosphate group, a carboxylic acid group, a sulfonic acid group, a hydroxy group, an amine group, a urea group, a guanidino group, and a disulfide group, and is the water-soluble carbon chain substance according to claim 56.
59. The binding portion is one or more selected from a divalent fatty acid or a polyvalent fatty acid, an amino acid, a targeting protein, a targeting polypeptide, and a targeting polysaccharide, and is the water-soluble carbon chain substance according to any one of claims 56 to 58.
60. The water-soluble carbon chain substance is a compound, a complex, or a mixture, and is the water-soluble carbon chain substance according to any one of claims 56 to 59.
61. The water-soluble carbon chain substance according to claim 60 is a complex formed by linking a fatty acid having 3 to 50 carbon atoms and a water-soluble amino acid, a complex formed by linking a fatty acid having 3 to 50 carbon atoms to a targeting polypeptide, a complex formed by reacting a fatty acid having 3 to 50 carbon atoms, a targeting polypeptide, and PEG, or a complex formed by reacting a surfactant with one or more selected from dibasic fatty acids or polybasic fatty acids, amino acids, targeting proteins, targeting polypeptides, and targeting polysaccharides.
62. The saturated and / or unsaturated fatty acid is selected from saturated or unsaturated fatty acids having 3 to 50 carbon atoms, and the fatty acid contains a double bond, a triple bond, a hydroxy group, an amino group, and / or is a fatty acid or amino acid substituted with oxygen, and is a monobasic acid, a dibasic acid, or a polybasic acid. The water-soluble carbon chain substance according to any one of claims 56 to 60.
63. The saturated and / or unsaturated fatty acid is a saturated fatty acid having 3 to 46 carbon atoms, a monoenoic acid having 3 to 34 carbon atoms, a dienoic acid having 5 to 30 carbon atoms, a trienoic acid having 7 to 30 carbon atoms, a tetraenoic acid having 12 to 38 carbon atoms, a pentaenoic acid having 12 to 38 carbon atoms, a hexaenoic acid having 22 to 38 carbon atoms, an acetylenic acid having 6 to 22 carbon atoms, a diacetylenic acid having 10 to 22 carbon atoms, a triacetylenic acid having 12 to 22 carbon atoms, an enynoic acid having 8 to 20 carbon atoms, a fatty acid having a main chain carbon number of 3 to 30 and a branched carbon number of 1 to 10 and / or 1 to 3 hydroxy groups, a saturated linear and branched dicarboxylic acid and tricarboxylic acid having 3 to 38 carbon atoms, an unsaturated linear or branched dicarboxylic acid and tricarboxylic acid having 4 to 18 carbon atoms which may be substituted with a hydroxy group, a carboxylic acid substituted with an amino group, a hydroxy group, an oxo group, and / or a methyl group having 3 to 18 carbon atoms, an N-fatty acyl amino acid having 6 to 30 carbon atoms, an amino acid containing two or more fatty acyls, and a polycarboxylic acid linked by a thioether bond and an amide bond. The water-soluble carbon chain substance according to claim 62, which is one or more selected.
64. The saturated and / or unsaturated fatty acid is one or more selected from fumaric acid, caprylic acid, octenoic acid, glutaconic acid, hexanoic acid, suberic acid, nonanoic acid, dodecanoic acid, dodecanedioic acid, tridecanoic acid, tridecanedioic acid, tetradecanoic acid, hexadecanoic acid, hexadecanedioic acid, octadecanoic acid, eicosanoic acid, eicosanedioic acid, oleic acid, linoleic acid, linolenic acid, eicosapentaenoic acid, cetoleic acid, docosapentaenoic acid, docosahexaenoic acid, pentacosanoic acid, enanthic acid, decanoic acid, undecylenic acid, dodecenoic acid, tetradecenoic acid, hexadecenoic acid, triacontenoic acid, dotriacontanehexaenoic acid, octacosanoic acid, or a carbon chain residue formed by these, and is the water-soluble carbon chain substance according to claim 62.
65. The water-soluble portion is a molecule or a residue of a molecule containing one or more groups selected from a mercapto group, an amino group, a carboxylic acid group, a hydroxy group, and a disulfide group, and the molecule is one or more water-soluble macromolecules or residues thereof selected from proteins, polysaccharides, nucleic acids, and artificially synthesized water-soluble polymers, and / or one or more medium molecules or residues thereof selected from polypeptides, oligopeptides, oligosaccharides, oligonucleotides, and artificially synthesized medium molecular weight water-soluble polymers, and / or one or more water-soluble small molecules or residues thereof selected from amino acids, monosaccharides, disaccharides, nucleotides, water-soluble vitamins, and deoxyribonucleotides, and / or a molecule or a residue of a molecule linked to the carbon chain that is the active portion, and the molecule or the residue of the molecule contains one or more groups selected from a mercapto group, an amino group, a carboxylic acid group, a hydroxy group, and a disulfide group, and is the water-soluble carbon chain substance according to any one of claims 56 to 60.
66. The protein, which is the water-soluble macromolecule, is one or more water-soluble macromolecules selected from serum albumin, immunoglobulin, water-soluble collagen, chaperone, water-soluble glycoprotein, and CD14; the polysaccharide, which is the macromolecule, is one or more water-soluble macromolecules selected from glucan, hyaluronic acid, sialic acid, heparin sulfate, heparan sulfate, chondroitin sulfate, dermatan sulfate, keratan sulfate, acetylated water-soluble cellulose derivative, β-cyclodextrin and its derivatives, and water-soluble chitosan derivative; the water-soluble polymer, which is the macromolecule, is one or more water-soluble macromolecules selected from polyethylene glycol and carboxylated or aminated polyethylene glycol, polyvinyl alcohol and carboxylated or quaternized polyvinyl alcohol, polyacrylic acid, and ammonium polyacrylate. The medium-molecular-weight water-soluble polymer is one or more substances selected from targeting polypeptide, oligopeptide, oligosaccharide, oligonucleotide, and / or water-soluble polyamino acid. The water-soluble small-molecule monosaccharide and / or disaccharide is one or more selected from glucose, fructose, rhamnose, sorbose, sucrose, maltose, lactose, and trehalose; the nucleotide and / or deoxyribonucleotide, which is the water-soluble small molecule, is selected from adenylate, guanylate, uridylate, cytidylate, thymidylate, inosine, deoxyadenylate, deoxyguanylate, deoxycytidylate, and deoxythymidylate; the amino acid, which is the water-soluble small molecule, is one or more selected from serine, threonine, cysteine, asparagine, glutamine, tyrosine, lysine, arginine, histidine, aspartic acid, glutamic acid, citrulline, ornithine, taurine, and aminobutyric acid; the vitamin, which is the water-soluble small molecule, is one or more selected from vitamin B1, pantothenic acid, vitamin B6, and vitamin C. The water-soluble carbon chain substance according to claim 65.
67. The targeting polypeptide contains any one of specific targeting microbial lipid membranes, bacterial and fungal cell walls, proteins of viral surface protein domains, or neutralizing antibody fragments. The water-soluble carbon chain substance according to claim 66.
68. The water-soluble polyamino acid is selected from polyglutamic acid, polylysine, and / or polyaspartic acid, and is the water-soluble carbon chain substance according to claim 66.
69. The binding moiety is the same as the water-soluble moiety, i.e., a protein, polypeptide, oligopeptide, oligosaccharide, monosaccharide, disaccharide, amino acid, nucleotide, vitamin, water-soluble polymer, water-soluble polyamino acid, and / or polysaccharide molecule or a residue of these molecules that can bind to a microbial lipid membrane, the cell membrane of an animal or human tissue, or the cell membrane surface domain. The molecule or the residue of the molecule contains one or more groups selected from a mercapto group, an amino group, a carboxylic acid group, a hydroxy group, and a disulfide group, and is the water-soluble carbon chain substance according to claim 56.
70. A compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms with at least one selected from proteins, polypeptides, oligopeptides, oligosaccharides, monosaccharides, disaccharides, nucleotides, vitamins, amino acids, water-soluble polymers, water-soluble polyamino acids, and polysaccharide molecules, or a mixture of a compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms with at least one selected from proteins, polypeptides, oligopeptides, oligosaccharides, monosaccharides, disaccharides, nucleotides, vitamins, amino acids, water-soluble polymers, water-soluble polyamino acids, and polysaccharide molecules, and the unreacted fatty acid and / or the unreacted protein, polypeptide, oligopeptide, oligosaccharide, monosaccharide, disaccharide, nucleotide, vitamin, amino acid, water-soluble polymer, water-soluble polyamino acid, and / or polysaccharide molecule, and is the water-soluble carbon chain substance according to claim 56.
71. A complex obtained by complexing a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms with at least one selected from proteins, polypeptides, oligopeptides, oligosaccharides, monosaccharides, disaccharides, nucleotides, vitamins, amino acids, water-soluble polymers, water-soluble polyamino acids, and polysaccharide molecules by physicochemical action, or a mixture directly physically mixed, wherein the physicochemical action includes hydrogen bonding or van der Waals forces or a combination of both of these actions, and is the water-soluble carbon chain substance according to claim 56.
72. A compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms with at least one selected from proteins, polypeptides, oligopeptides, and amino acids, or a mixture of a compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms with at least one selected from proteins, polypeptides, oligopeptides, and amino acids and at least one selected from unreacted fatty acids and / or unreacted proteins, polypeptides, oligopeptides, and amino acids, the water-soluble carbon chain substance according to claim 70.
73. A compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms, PEG, and at least one selected from proteins, polypeptides, oligopeptides, and amino acids, or a mixture of a compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms, PEG, and at least one selected from proteins, polypeptides, oligopeptides, and amino acids and at least one selected from unreacted fatty acids, unreacted PEG, and / or unreacted proteins, polypeptides, oligopeptides, and amino acids, the water-soluble carbon chain substance according to claim 70.
74. A compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms with at least one selected from polysaccharides, monosaccharides, disaccharides, and oligosaccharides, or a mixture of a compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms with at least one selected from polysaccharides, monosaccharides, disaccharides, and oligosaccharides and unreacted fatty acids and / or unreacted polysaccharides, monosaccharides, disaccharides, and / or oligosaccharides, the complex according to claim 70.
75. A compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms, PEG, and at least one selected from polysaccharides, monosaccharides, disaccharides, and oligosaccharides, or a mixture of a compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms, PEG, and at least one selected from polysaccharides, monosaccharides, disaccharides, and oligosaccharides and unreacted fatty acids, unreacted PEG, and / or unreacted polysaccharides, monosaccharides, disaccharides, and / or oligosaccharides, the water-soluble carbon chain substance according to claim 70.
76. The water-soluble carbon chain substance according to claim 70 or 71, wherein the protein is one or more selected from serum albumin, immunoglobulin, water-soluble collagen, chaperone, water-soluble glycoprotein, and CD14.
77. The water-soluble carbon chain substance according to claim 70 or 71, wherein the polysaccharide is one or more selected from glucan and / or hyaluronic acid, sialic acid, heparin sulfate, heparan sulfate, chondroitin sulfate, dermatan sulfate, keratan sulfate, acetylated water-soluble cellulose derivative, β-cyclodextrin and its derivatives, and water-soluble chitosan derivatives.
78. A compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms, a linker, and a protein containing a mercapto group, or a mixture of a compound obtained by the above reaction, unreacted fatty acid, unreacted linker, and / or a protein containing an unreacted mercapto group, wherein the linker is one or more of amino acid, succinic acid, butadienoic acid, glutaconic acid, hexamiminodiacid, urethane, short peptide, N-hydroxybutenimide, polyethylene glycol, and derivatives of the above compounds. The water-soluble carbon chain substance according to claim 70.
79. A compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms, N-hydroxybutenimide, and a protein containing a mercapto group, or a mixture of a compound obtained by the above reaction, unreacted fatty acid, unreacted N-hydroxybutenimide, and / or a protein containing an unreacted mercapto group. The water-soluble carbon chain substance according to claim 78.
80. A compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 100 carbon atoms, cystamine, and at least one selected from polysaccharides, monosaccharides, disaccharides, and oligosaccharides, or a compound obtained by reacting a saturated and / or unsaturated fatty acid having 3 to 50 carbon atoms, cystamine, and at least one selected from polysaccharides, monosaccharides, disaccharides, and oligosaccharides, and a mixture of unreacted fatty acid, at least one selected from unreacted polysaccharides, monosaccharides, disaccharides, and oligosaccharides, and / or unreacted cystamine. The water-soluble carbon chain substance according to claim 70.
81. The compound obtained by the reaction contains one or more groups selected from an amide group, an ester group, a thioether group, or an ether group, and these groups function as a part for linking a water-soluble part and an active part. The water-soluble carbon chain substance according to any one of claims 70 to 80.
82. The saturated and / or unsaturated fatty acid has 3 to 50 carbon atoms, preferably 3 to 48 carbon atoms, more preferably 3 to 30 carbon atoms, and still more preferably 3 to 26 carbon atoms. The water-soluble carbon chain substance according to any one of claims 56 to 81.
83. The saturated and / or unsaturated fatty acid is a fatty acid having 3 to 40 carbon atoms containing 1 to 8 C═C double bonds, a fatty acid containing 1 to 7 C═C double bonds, a fatty acid containing 1 to 6 double bonds, a fatty acid containing 1 to 5 double bonds, a fatty acid containing 1 to 4 double bonds, a fatty acid containing 1 to 3 double bonds, or a fatty acid containing 1 to 2 double bonds. Preferably, the saturated and / or unsaturated fatty acid is a fatty acid having 1 to 6 double bonds and 3 to 30 carbon atoms. The water-soluble carbon chain substance according to any one of claims 70 to 81.
84. The saturated and / or unsaturated fatty acid has 3 to 30 carbon atoms. The water-soluble carbon chain substance according to any one of claims 56 to 81.
85. The saturated and / or unsaturated fatty acid is one or more fatty acids selected from fumaric acid, caprylic acid, octenoic acid, glutaconic acid, hexanoic acid, suberic acid, nonanoic acid, dodecanoic acid, dodecanedioic acid, tridecanoic acid, tridecanedioic acid, tetradecanoic acid, hexadecanoic acid, hexadecanedioic acid, octadecanoic acid, eicosanoic acid, eicosanedioic acid, oleic acid, linoleic acid, linolenic acid, eicosapentaenoic acid, cetoleic acid, docosapentaenoic acid, docosahexaenoic acid, pentacosanoic acid, enanthic acid, decanoic acid, undecylenic acid, dodecenoic acid, tetradecenoic acid, hexadecenoic acid, triacontenoic acid, dotriacontanehexaenoic acid, octacosanoic acid. The water-soluble carbon chain substance according to any one of claims 56 to 81.
86. The protein is human serum protein or bovine serum protein, or CD14, or the polysaccharide is glucan and / or hyaluronic acid, and the water-soluble carbon chain substance according to any one of claims 56 to 81.
87. The compound obtained by the reaction is a compound obtained by a fatty acid, albumin, or SBP1 reaction, and has one or more of the following structural formulas, and the water-soluble carbon chain substance according to claim 72. 【Chemical 19】 【Chemical 20】 【Chemical 21】
88. The compound obtained by the reaction is a compound obtained by reacting a monovalent fatty acid having 3 to 10 carbon atoms, PEG, and an amino acid, or a compound obtained by reacting a monovalent fatty acid having 3 to 10 carbon atoms, a saturated divalent fatty acid having 5 to 8 carbon atoms, PEG, and taurine, and the water-soluble carbon chain substance according to claim 73.
89. The compound obtained by the reaction is a compound having at least one of the following structural formulas, 【Chemical 22】 n is an integer from 1 to 200, and the water-soluble carbon chain substance according to claim 88.
90. The compound obtained by the reaction is one or more compounds having the following structural formulas obtained by reacting a fatty acid and glucan, and the water-soluble carbon chain substance according to claim 74. 【Chemical 23】 【Chemical 24】 【Chemical 25】 【Chemical 26】
91. The compound obtained by the reaction is one or more compounds having the following structural formulas obtained by reacting a fatty acid and hyaluronic acid, 【Chemical 27】 【Chemical Formula 28】 【Chemical 29】 【Chemical 30】 n is an integer from 1 to 2000, and the water-soluble carbon chain substance according to claim 74.
92. The compound obtained by the reaction is a compound obtained by reacting a fatty acid having 3 to 10 carbon atoms, PEG, and glucose, and the water-soluble carbon chain substance according to claim 75.
93. The compound obtained by the reaction is a compound having the following structural formula, 【Chemical 31】 n is an integer from 1 to 200, and the water-soluble carbon chain substance according to claim 92.
94. The compound obtained by the reaction is one or more compounds having the following structural formulas obtained by reacting a fatty acid, N-hydroxybutenimide, and a protein, and having a thioether bond, and the water-soluble carbon chain substance according to claim 79. 【Chemical 32】 【Chemical 33】 【Chemical 34】
95. The compound obtained by the reaction is one or more compounds having the following structural formulas obtained by reacting a fatty acid, cystamine, and glucan, and the water-soluble carbon chain substance according to claim 80. 【Chemical 35】 【Chemical 36】 【Chemical 37】
96. It contains small molecule compounds containing a hydroxy group and benzene rings, preferably, Flavon, Isoflavon, Anthocyanin, Soy Isoflavon, Aloe-emodin, Grape Seed Extract, Green Tea-derived Flavon, Naringenin, Limocitrin, Baicalein, Riboflavin, Quercetin, Graphite-derived Flavon, Sinzelenanin, Chrysin, Jujube Flavon, Morin, Luteolin, Mulberry Extract, Gypsum-derived Flavon, Honeysuckle-derived Flavon, Gentoflavin, Bellflower-derived Flavon, Violet-derived Flavon, Perilla-derived Flavon, Chrysanthemum-derived Flavon, Artemisinin, Red Peony-derived Flavon, Salvia-derived Flavon, Bupleurum-derived Flavon, Safflower-derived Flavon, Rock Jasmine-derived Flavon, Chinese Date-derived Flavon, Chinese Wolfberry-derived Flavon, Rehmannia Root-derived Flavon, Jujube-derived Flavon, Schisandra Chinensis-derived Flavon, Licorice-derived Flavon, Panax Notoginseng-derived Flavon, Curcumin, Apigenin, Carotene, Anthocyanidin, Lutein, Zeaxanthin, Wasabi Extract, Rutin, Scutellarein, Pollen Yellow Extract, Sage-derived Flavon, Goldenrod-derived Flavon, Cinnamon-derived Flavon, Isoflavonoid, and Anthocyanidin; Rutin, Emodin, Fucoxanthin, Gallic Acid, Persimmon Peel Extract, Morin, Echinacoside, Grape Seed-derived Procyanidin, Phenolic Acid, Tea Polyphenol, Naringin, Citric Acid, Flavonol, Glycyrrhizic Acid, Cinnamic Acid, Flavonoid Glycoside, Oleic Acid, Matrine, Tanshinone, Erythrophleine, Snadigmic Acid, Perillyl Alcohol, Anisic Acid, Amrencin, Hesperidin, Granatin, Morcin, Naringin, Linarin, Geniposide, Jasminosid, Naringetol, Carotene, Apigenin, Baimelin, Ginseng Extract, King Side, Chrysanthemum Extract, Olive Extract, Oolong Tea Extract, L-Theanine, Red Wine Extract, Bellflower Glycoside, Perilla Alcohol Glycoside, Moracin, Calthamin, Pinosin, Pakiminic Acid, Caffeic Acid, Chlorogenic Acid; Resveratrol, White Tea Polyphenol, Resveratrol Disaccharide, Banana-derived Lutein, Anthocyanidin, Arachidonic Acid, Peanut-derived Flavon, (+)-Piperitol, Anisofolin, Flavonoid, Baicalein, Flavonoid Glycoside, Flavanol, Red Wine Polyphenol, Rodiosin, Calphenol, Black Tea-derived Flavon, Sesamin, Rye Phenol, Fucitol, Seaweed Polysaccharides, Alginate, Farnesin, Cannabidiol, Polydatin,Cucurbitacin, fenugreek extract, cucurbitic acid, pollen phenol, pollen-derived flavone, pollen glycoside, pollen ester, arachidic acid, peanut-derived flavone glycoside, peanut isoflavone, peanut isoflavone glycoside, peanut isoflavone disaccharide, peanut isoflavone trisaccharide, peanut resveratrol, peanut resveratrol disaccharide, peanut resveratrol trisaccharide, peanut resveratrol tetrasaccharide, peanut resveratrol pentasaccharide, peanut resveratrol hexasaccharide, peanut resveratrol heptasaccharide, peanut resveratrol octasaccharide, peanut resveratrol nonasaccharide, peanut resveratrol decasaccharide, peanut resveratrol undecasaccharide, catechin, epicatechin, tea polyphenol, catechol, chlorophyll, protocatechuic acid, hesperidin, anthocyanidin, anthocyanin, anthocyanin, cyanidin alcohol, glucoside, glucopyranoside, tricin, soy isoflavone, flavanol, keltaninin, buckwheat sprout extract, persimmon peel extract, persimmon tannic acid, punica acid, granatin, blueberry extract, resveratrol, lycopene, naringenin, morin, chlorogenic acid, chlorogenic acid triglucoside, chlorogenic acid diglucoside, chlorogenic acid methyl, chlorogenic acid ethyl, chlorogenic acid propyl, chlorogenic acid butyl, chlorogenic acid isopropyl, chlorogenic acid hexyl, chlorogenic acid octyl, chlorogenic acid benzyl, chlorogenic acid phenethyl, chlorogenic acid phenylpropyl, chlorogenic acid phenylbutyl, chlorogenic acid phenylisopentyl, chlorogenic acid phenylhexyl, chlorogenic acid phenyloctyl, chlorogenic acid styryl, chlorogenic acid benzyl alcohol, chlorogenic acid phenylethanol, anthocyanidin, proanthocyanidin glycoside, and a water-soluble carbon chain substance according to any one of claims 56 to 69, comprising one or more substances selected from the group consisting of catechin.
97. The water-soluble carbon chain substance includes water-soluble medium and short-chain fatty acids, or fatty acid salts, or fatty acid derivatives, preferably, For example, water-soluble medium and short-chain fatty acids such as butyric acid, succinic acid, fumaric acid, valeric acid, glutaric acid, caproic acid, adipic acid, enanthic acid, pimelic acid, caprylic acid, octenoic acid, suberic acid, capric acid, sebacic acid; and, as fatty acid derivatives including any one or more of the following, such as surfactants, fatty acid salts, alkyl sulfonates, alkyl sulfates, alkyl phosphates, alkyl amine salts, alkyl quaternary ammonium salts, aliphatic acyl amino acids, betaines, fatty alcohol polyoxyethylene ethers, alkylphenol polyoxyethylene ethers, aliphatic amine polyoxyethylene ethers, polyol fatty acid esters, polyol polyoxyethylene ether fatty acid esters, fatty acid polyoxyethylene esters, alkyl polyglucosides, and alkyl ethoxypolyglucosides, one or more water-soluble medium and short-chain fatty acids, or fatty acid salts, or fatty acid derivative substances selected from the group consisting of, the water-soluble carbon chain substance according to any one of claims 56 to 69.
98. A preparation for regulating transmembrane transport of cell membranes, the structure or function of cell membranes, cell division and proliferation or cell migration and locomotion, cell aging, and / or the fluidity of cell membranes, prepared using the water-soluble carbon chain substance according to any one of claims 56 to 97.
99. The preparation according to claim 98, wherein the regulation of the fluidity of the cell membrane is an improvement in the fluidity of the cell membrane.
100. The preparation according to claim 98, wherein the regulation of the fluidity of the cell membrane is a decrease in the fluidity of the cell membrane.
101. The cell membrane includes a cytoplasmic membrane and an organelle membrane, the cell membrane or cell includes a cell membrane or cell of a microorganism, or a cell membrane or cell of a plant, animal or human tissue, the regulation includes increase or promotion, and inhibition or decrease, wherein the cell membrane of the microorganism includes the cell membranes of bacteria and fungi and the envelope of viruses. Here, the cell membrane structure includes a phospholipid bilayer, proteins adsorbed on the surface of the phospholipid bilayer, and polysaccharides embedded and inserted into the phospholipid bilayer. Specifically, it includes receptor proteins, transmembrane proteins, cytoskeletal proteins, and enzymes. Here, the transmembrane transport includes active transport, passive transport, endocytosis, and exocytosis, and the preparation according to claim 98.
102. The regulation of the transmembrane transport of the cell membrane includes an increase and promotion of the extracellular release of exosomes in the cell, and also includes the suppression or reduction of the extracellular release of exosomes in the cell, and prevents the entry of viruses into the cell. The suppression or reduction of the transmembrane transport of the virus suppresses or reduces the entry of the virus into the cell through the endocytosis effect, or suppresses or reduces the entry of the virus into the cell through the fusion of the virus envelope and the cell membrane. It is used for all of the prevention of virus infection, the prevention of mycoplasma and chlamydia infection, and the prevention of bacterial infection. The substances transported through the cell membrane include at least one or two or more of small molecule compounds, medium molecule compounds, large molecule compounds, viruses, bacteria, pathogenic microorganisms such as mycoplasma, chlamydia, and fungi, and nanoparticles and nanodrugs. The preparation according to claim 98.
103. The preparation for improving the fluidity of the cell membrane among the above preparations includes preparations for drug delivery, gene transfection, cell therapy, diabetes, improvement of the nervous system, improvement of Alzheimer's disease, strengthening of the immune system, hypercholesterolemia, and / or prevention, prevention, improvement and / or treatment of inflammatory bowel disease. The preparation according to claim 99.
104. The preparation for reducing the fluidity of the cell membrane among the above preparations includes preparations for the prevention, prevention, improvement and / or treatment of cardiovascular diseases (including coronary heart disease, hypertension, myocardial infarction, heart failure), obesity, autism, osteoporosis, inflammatory diseases, autoimmune diseases, chronic fatigue syndrome, leukemia, autolysis of self-cells, virus infection and / or neurodegenerative diseases. The preparation according to claim 100.
105. A preparation for preventing, preventing or treating microbial infection prepared using the water-soluble carbon chain substance according to any one of claims 56 to 97.
106. The preparation is a pharmaceutical preparation or an environmental disinfection preparation, and the pharmaceutical preparation is preferably one selected from the group consisting of inhalants, nasal sprays, injections, oral preparations, and topical skin dosage forms, the preparation according to claim 98.
107. Use of the water-soluble carbon chain substance according to any one of claims 56 to 97 in the preparation of a pharmaceutical preparation or an environmental disinfection microbial reagent for preventing, inhibiting and / or treating microbial infections, preferably, the microorganism is any one or two selected from the group consisting of viruses, bacteria, and fungi, the virus is an enveloped virus and / or a non-enveloped virus, more preferably, the virus is one or more viruses selected from the group consisting of novel coronavirus, influenza virus, human immunodeficiency virus (HIV), hepatitis B virus, human herpes virus, Ebola virus, rabies virus, and human papillomavirus (HPV), the bacteria is one or more bacteria selected from the group consisting of Escherichia coli, Staphylococcus aureus, methicillin-resistant Staphylococcus aureus, Streptococcus pneumoniae, Klebsiella pneumoniae, and Pseudomonas aeruginosa, still more preferably, the virus is one or more selected from the group consisting of H7N9 influenza virus, H5N1 influenza virus, HIV virus, novel coronavirus, HPV virus, and rabies virus, use.
108. The use according to claim 107, wherein the water-soluble carbon chain substance according to any one of claims 56 to 95 is prepared into a solution with a concentration of 0.2 mM to 10 mM when acting on microorganisms.
109. The use according to claim 107, which is prepared into a solution with a concentration of 0.5 mM to 10 mM.
110. A preparation for preventing, inhibiting or treating inflammatory reactions and / or body aging, prepared using the water-soluble carbon chain substance according to any one of claims 56 to 97.
111. The preparation according to claim 110, wherein the prevention of body aging includes the prevention of skin aging, and the prevention, inhibition or treatment of the inflammatory reaction includes changing the three-dimensional structure of inflammatory factors (proteins).
112. The preparation according to claim 110, wherein the carbon chain substance binds oxygen radicals.
113. The carbon chain substance is Flavon, Isoflavon, Anthocyanin, Soybean Isoflavon, Aloesin, Grape Seed Extract, Green Tea-derived Flavon, Naringenin, Limocitrin, Baicalein, Riboflavin, Quercetin, Graphite-derived Flavon, Sinzelenanin, Chrysin, Japanese Apricot Flavon, Morin, Luteolin, Mulberry Extract, Gypsum-derived Flavon, Honeysuckle-derived Flavon, Gentoflavin, Bellflower-derived Flavon, Violet-derived Flavon, Perilla-derived Flavon, Chrysanthemum-derived Flavon, Artemisinin, Red Peony-derived Flavon, Salvia-derived Flavon, Bupleurum-derived Flavon, Safflower-derived Flavon, Rock Jasmine-derived Flavon, Jujube-derived Flavon, Chinese Wolfberry-derived Flavon, Rehmannia Root-derived Flavon, Jujube Seed-derived Flavon, Schisandra Fruit-derived Flavon, Licorice-derived Flavon, Panax Notoginseng-derived Flavon, Curcumin, Apigenin, Carotene, Anthocyanidin, Lutein, Zeaxanthin, Horseradish Extract, Rutin, Scutellarein, Pollen Yellow Extract, Sage-derived Flavon, Dandelion-derived Flavon, Cinnamon-derived Flavon, Isoflavonoid, and Anthocyanidin; Rutin, Emodin, Fucoxanthin, Gallic Acid, Persimmon Peel Extract, Morin, Echinacoside, Grape Seed-derived Procyanidin, Phenolic Acid, Tea Polyphenol, Naringin, Citric Acid, Flavonol, Glycyrrhizic Acid, Cinnamic Acid, Flavonoid Glycoside, Oleic Acid, Matrine, Tanshinone, Erythrophleine, Snadigmic Acid, Perillyl Alcohol, Anisic Acid, Amrencin, Hesperidin, Granatin, Morsin, Naringin, Linarin, Gentiopicroside, Jasminosid, Naringetol, Carotene, Apigenin, Baimelin, Scutellaria Baicalensis Georgi Extract, Kingoside, Chrysanthemum indicum Extract, Olive Extract, Oolong Tea Extract, L-Theanine, Red Wine Extract, Bellflower Glycoside, Perilla Alcohol Glycoside, Moracin, Caltaemin, Pinosin, Pakiminic Acid, Caffeic Acid, Chlorogenic Acid; Resveratrol, White Tea Polyphenol, Resveratrol Disaccharide, Banana-derived Lutein, Anthocyanidin, Arachidonic Acid, Peanut-derived Flavon, (+)-Piperitol, Anisofolin, Flavonoid, Baicalein, Flavonoid Glycoside, Flavanol, Red Wine Polyphenol, Rhodiocyan, Calphenol, Black Tea-derived Flavon, Sesamin, Rye Phenol, Fucitol, Seaweed Polysaccharides, Alginate, Farnesin, Cannabidiol, Polydatin,Kukurbitacin, fenugreek extract, cucurbitic acid, pollen phenol, pollen-derived flavonoid, pollen glycoside, pollen ester, arachidic acid, peanut-derived flavonoid glycoside, peanut isoflavone, peanut isoflavone glycoside, peanut isoflavone disaccharide, peanut isoflavone trisaccharide, peanut resveratrol, peanut resveratrol disaccharide, peanut resveratrol trisaccharide, peanut resveratrol tetrasaccharide, peanut resveratrol pentasaccharide, peanut resveratrol hexasaccharide, peanut resveratrol heptasaccharide, peanut resveratrol octasaccharide, peanut resveratrol nonasaccharide, peanut resveratrol decasaccharide, peanut resveratrol undecasaccharide, catechin, epicatechin, tea polyphenol, catechol, chlorophyll, protocatechuic acid, hesperidin, anthocyanidin, anthocyanin, anthocyanin, cyanidin alcohol, glucoside, glucopyranoside, tricin, soybean isoflavone, flavanol, keltaninin, buckwheat leaf extract, persimmon peel extract, persimmon tannic acid, punica acid, granatin, blueberry extract, resveratrol, lycopene, naringenin, morin, chlorogenic acid, chlorogenic acid triglucoside, chlorogenic acid diglucoside, chlorogenic acid methyl, chlorogenic acid ethyl, chlorogenic acid propyl, chlorogenic acid butyl, chlorogenic acid isopropyl, chlorogenic acid hexyl, chlorogenic acid octyl, chlorogenic acid benzyl, chlorogenic acid phenethyl, chlorogenic acid phenylpropyl, chlorogenic acid phenylbutyl, chlorogenic acid phenylisopentyl, chlorogenic acid phenylhexyl, chlorogenic acid phenyloctyl, chlorogenic acid styryl, chlorogenic acid benzyl alcohol, chlorogenic acid phenylethanol, anthocyanidin, proanthocyanidin glycoside, and a preparation according to claim 110, which binds one or more substances selected from the group consisting of catechin, or the carbon chain substance is one or more substances selected from the group consisting of the above substances, or the carbon chain substance is mixed with one or more substances selected from the group consisting of the above substances to prepare a formulation.
114. When the preparation is used for the prevention, inhibition or treatment of inflammatory reactions and / or the aging of the body, the water-soluble carbon chain substance is prepared in a solution with a concentration of 0.1 nM to 5 mM. Preferably, the carbon chain substance is a complex formed by a fatty acid and an amino acid. More preferably, the concentration of the complex solution is 0.1 nM to 300 μM, and even more preferably 5 nM to 100 μM. The preparation according to any one of claims 110 to 113.
115. When the preparation is used for the prevention, inhibition or treatment of inflammatory reactions and / or the aging of the body, the water-soluble carbon chain substance is prepared in a solution with a concentration of 0.1 nM to 300 μM, preferably 5 nM to 100 μM. The preparation according to claim 114.
116. A pharmaceutical preparation for preventing, inhibiting, alleviating or treating neurodegenerative diseases, prepared using the water-soluble carbon chain substance according to any one of claims 56 to 97.
117. The neurodegenerative disease includes Alzheimer's disease (AD), Parkinson's disease (PD), Huntington's disease (HD), Alzheimer's disease, amyotrophic lateral sclerosis (ALS), various types of spinocerebellar ataxia (SCA), or Pick's disease. The pharmaceutical preparation according to claim 116.
118. The water-soluble carbon chain substance is prepared in a solution with a concentration of 0.1 nM to 5 mM to exert its effect. The pharmaceutical preparation according to claim 116.
119. The water-soluble carbon chain substance is prepared in a solution with a concentration of 0.1 nM to 300 μM, preferably 5 nM to 100 μM to exert its effect. The pharmaceutical preparation according to claim 116.
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