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Compound for preventing, preventing or treating microbial infection as well as preparation method and application thereof

A compound and microbial technology, applied in the field of bacteria, preventable treatment of viruses, preventive treatment of viruses, fungal infectious diseases, and complexes of bacterial and fungal infections, can solve the problem of not being able to be widely killed and prevented, and the lack of antibacterial Toxic side effects and other issues

Active Publication Date: 2022-06-03
太阳雨林(北京)生物医药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0043] The present invention aims at the lack of non-toxic side effects in the prior art and cannot widely kill and prevent, prevent or treat microbial infections, and provides a kind of agent that can prevent, prevent or treat microbial infections Complex for the treatment of microbial infections
[0044] Specifically, in order to solve the lack of non-toxic side effects in the prior art, especially reagents that cannot extensively kill and prevent, prevent or treat microbial infections, the present invention provides the following The first set of technical solutions:

Method used

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  • Compound for preventing, preventing or treating microbial infection as well as preparation method and application thereof
  • Compound for preventing, preventing or treating microbial infection as well as preparation method and application thereof
  • Compound for preventing, preventing or treating microbial infection as well as preparation method and application thereof

Examples

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preparation example Construction

[0266] The complex of the present invention is prepared by combining a carbon chain-providing compound such as a fatty acid with proteins, polypeptides, oligopeptides, oligosaccharides, monosaccharides, disaccharides, oligonucleotides, vitamins, water-soluble polymers, water-soluble Polyamino acids and / or polysaccharide molecules react, or add linkers such as PEG, N-hydroxybutenimide, amino acids, succinic acid, butadienoic acid, glutaric acid, hexamethylene diacid, Any one or two or more of carbamates, short peptides, etc. and their derivatives are reacted to obtain a reaction mixture; in a preferred scheme, the reaction mixture is further purified to separate and obtain a purified reaction product (in The "purified reaction product" is also referred to as "reaction-obtained compound" in this application, and the term "reaction-obtained compound" refers to the substance remaining after the reaction mixture is separated by purification means to remove unreacted substances, whic...

Embodiment 1

Example 1 Preparation and characterization of human serum albumin / bovine serum albumin grafted fatty acid complex (acting part + macromolecular water-soluble part / binding part)

The reaction formula example 1-1 is as follows:

In this embodiment, the molar ratio of fatty acid and albumin is 10:1, and the fatty acid is selected from fumaric acid, octanoic acid, undecanoic acid, hexadecenoic acid, oleic acid, linoleic acid, linolenic acid and eicosapentaenoic acid respectively. (EPA), docosahexaenoic acid (DHA), and triaconoic acid react with serum albumin, respectively. The molar ratio of catalyst to fatty acid is 1:1, and the catalyst is 1-ethyl-(3-dimethylaminopropyl) carbodiimide (EDC), N-hydroxysulfosuccinimide (sulfo-NHS) . The reaction process is as follows:

Accurately weigh 0.36 mmol of fatty acid, 0.36 mmol of EDC, and 0.36 mmol of sulfo-NHS; add acid to catalyze and activate the carboxyl group to form activated fatty acid; stir and activate under ice bath for 15...

Embodiment 2

[0322] Example 2 Preparation and characterization of bovine serum albumin grafted fatty acid complex (acting part + macromolecular water-soluble part / binding part)

Accurately weigh 0.36 mmol of oleic acid; 0.36 mmol of EDC; 0.36 mmol of sulfo-NHS with acid to catalyze and activate the carboxyl group to obtain activated oleic acid; stir and activate under ice bath for 10 min. Precisely weigh 0.018 mmol of bovine serum albumin (calculated as 1.2 g by mass), dissolve it in 5 ml of PBS solution, add NaOH solution to adjust the pH to neutrality, and stir evenly to obtain a serum albumin solution. The serum albumin solution was added to the activated oleic acid under stirring, and the stirring reaction was continued overnight in an ice bath to obtain the initial dissolution of oleic acid-albumin with an oleic acid concentration of 72 mM. The above solution was precipitated with ice acetone, then ethanol was used to remove fatty acids that did not participate in the reaction, and sm...

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Abstract

The invention relates to a compound for preventing, preventing or treating microbial infection as well as a preparation method and application thereof. The compound comprises an acting part, a binding part and a water-soluble part, the acting part is a fat-soluble saturated and / or unsaturated carbon chain with a branched chain, a ring structure and / or a straight chain structure, and can be inserted into / fused into a lipid membrane of a microorganism to destroy the lipid membrane or wrap non-enveloped viruses to realize hydrophobic isolation; the binding part can be bound with a lipid membrane component or a virus surface protein structural domain, so that the compound is connected to a lipid membrane or a virus surface, and the compound can also have specific targeting lipid membrane component or virus surface protein structural domain to endow targeting property; the water-soluble part enables the compound to be uniformly dispersed in an aqueous solution and prevents the acting part from being gathered into clusters. The compound can be prepared into various dosage forms, can be used for preventing or preventing infection of microorganisms such as viruses, bacteria and fungi before infection, can be used for killing the microorganisms in the body after infection, and can also be used for killing the environment to prevent spreading of the viruses, the bacteria and the fungi.

Description

technical field [0001] The present invention relates to the field of pharmacy, more particularly, to a group of complexes that can prevent and treat viral, bacterial and fungal infections, and a preparation method of the complexes. application in disease. Background technique [0002] Among many microorganisms, the pathogenic microorganisms that can directly cause human diseases are generally viruses, bacteria and fungi. Except for a few non-enveloped viruses, most microorganisms have lipid membranes, and the lipid membranes of microorganisms have the same function as the cell membranes of other organisms. attached to the surface of the phospholipid bilayer. There are proteins on the outer surface of the membrane, glycoproteins composed of a small amount of polysaccharides, and some carbohydrates are combined with lipids to form glycolipids. The lipid membrane of microorganisms is usually 7~8nm and has a certain fluidity. It not only acts as a barrier to create a stable i...

Claims

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Application Information

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IPC IPC(8): A61K45/00A61K31/20A61K31/201A61K47/54A61K47/61A61K47/64A61P31/04A61P31/10A61P31/12
CPCA61K47/64A61K47/61A61K47/542A61K47/549A61K47/545A61K31/201A61K31/20A61K45/00A61K47/643A61P31/04A61P31/10A61P31/12A61P31/16A61P31/20A61P31/18A61P31/22Y02A50/30
Inventor 赵一麟周媛媛刘凤武周旭陈炜斌刘弘毅
Owner 太阳雨林(北京)生物医药有限公司