146 results about "Bioactive molecules" patented technology

The invention provides a nucleic acid aptamer and a screening method thereof, the aptamer is of an oligonucleotide DNA structure, the nucleotide sequence of the nucleic acid aptamer is the nucleotide sequence of any DNA fragment as shown in SEQ ID NO: 1-9, and the nucleic acid aptamer can specifically target cardiac muscle cells (CMs). According to the invention, a new strategy can be provided for clinical treatment of cardiovascular diseases, and meanwhile, bioactive molecules such as microRNA (miRNA), small interfering RNA (small interfering RNA, siRNA), lipidosome, microspheres, microcapsules and the like can be carried to be used as an intracellular drug delivery tool.

We are disclosing derivatives of 5-hydroxylated polymethoxyflavones. The derivatives offer enhanced oral bioavailability and improved intestinal permeability. The derivatives of the invention release the biologically active 5-hydroxylated polymethoxyflavones that are activated by chemical or enzymatic processes in the GI Tract. The derivatives are constructed as bioreversible prodrugs containing the bioactive molecules covalently linked with lipids like fatty acids, glycerides or phospholipids. The derivatives are useful against inflammatory conditions and aging. Formulations including the derivatives are also disclosed.

The invention belongs to the field of tendon tissue scaffold preparation, and provides a tendon tissue scaffold preparation method based on a decellularization technology. Although the existing decellularization technology can realize removal of cell components and retention of a matrix structure, contradiction still exists in the aspects of considering decellularization efficiency and matrix integrity. The method comprises three steps of freeze thawing treatment, trypsin digestion ultrasonic treatment and nuclease treatment, and perfect balance between decellularization efficiency and matrix retention is realized by optimizing freeze thawing parameters, regulating ultrasonic conditions and reasonably matching enzyme types and concentrations. According to the method, the cell structure can be accurately destroyed, the release of cell contents is promoted, and meanwhile, the extracellular matrix structure and bioactive molecules are protected. Experiments show that the tendon tissue scaffold prepared by the invention is thorough in cell removal, retains an extracellular matrix structure of natural tendons to the greatest extent, is closer to natural tissues in mechanical properties and biological functions, and provides a new thought for tendon repair research and application.

The present disclosure relates to biologically active molecules comprising a single domain antibody (sdAb) that specifically binds to the extracellular domain of human gp130, compositions comprising such antibodies, and methods of use thereof.

An injectable liquid containing bioactive molecules released from a powder comprising a neo-synthesized extracellular matrix for use in the treatment or prevention of cancer, in particular in the local treatment of solid tumors.

A pharmaceutical combination for subcutaneous administration and use thereof are provided. The pharmaceutical combination as described herein for subcutaneous administration includes a hyaluronidase and an antibody-drug conjugate. The antibody-drug conjugate includes a fragment of a bioactive molecule, and the bioactive molecule has moderate toxicity. The pharmaceutical combination can achieve a larger volume and a larger dose of administration, and the side reaction is not enhanced.

The invention discloses a fresh-keeping storage method of plum fruits, which is characterized in that a compact network structure of a shellac-pullulan-gellan gum basic composition effectively obstructs invasion of external microorganisms, and significantly slows down loss of water in the fruits, so that the plump appearance and hardness of the fruits are maintained, and the fruit quality is improved. The siRNA and the AVG wrapped by the lipidosome accurately interfere with the ripening and senescence process in the fruit from the molecular level, the siRNA specifically silences the gene expression of cell wall degradation key enzyme and delays the softening process of the fruit, and the AVG effectively blocks the biosynthesis pathway of ethylene and inhibits the start of an after-ripening signal, so that the ripening and senescence process of the fruit is delayed. The external formed physical film provides a stable microenvironment for internal bioactive molecules, protects the internal bioactive molecules from being degraded and prolongs the action time, and the internal molecular regulation delays the disintegration of cell structures, so that the external film can be attached more enduringly and exerts a barrier function, and the maintenance of the fruit quality is realized under a refrigeration condition.

Phthalide lactones, as an important class of benzopentolactone skeleton, are widely distributed in natural products, medicinal plants and bioactive molecules, and have significant pharmacological activities and synthetic application potential. This kind of structure not only shows various biological activities such as antibacterial, anti-inflammatory, antitumor, antioxidant, but also is an indispensable core structural unit in many drug molecules and lead compounds. At the same time, cyano is a very valuable functional group in the field of organic synthesis and medicinal chemistry, with strong electron-withdrawing properties, strong structural stability and other advantages, which can effectively improve the electronic distribution, lipid solubility and drug performance of the molecule. In view of the important significance of phthalide lactones and cyano in organic synthesis and drug research and development, the present invention develops a synthetic method for efficiently constructing cyano-containing alkyl chain substituted phthalide lactone compounds. It has important value in medicinal chemistry and organic synthesis.

The application discloses a tetra-substituted furanone compound and a preparation method and application thereof. The structural formula of the tetra-substituted furanone compound is shown in formula (III); wherein, R 1 is an aromatic group, a substituted aromatic group, an alkyl group or a substituted alkyl group; 2 R 3 is an aromatic group, a substituted aromatic group, an alkyl group, a substituted alkyl group or a heterocyclic group; R 4 is an aromatic group, a substituted aromatic group, an alkyl group, a substituted alkyl group or a heterocyclic group. The tetra-substituted furanone compound provided by the application is widely distributed in natural products and bioactive molecules, and can be used as a multi-purpose intermediate and precursor in organic synthesis. The tetra-substituted furanone compound is also a potential strong antiviral active molecule, and has a wide application prospect in the field of antiviral drug research and development.

The invention provides a B cell or CD11b + cell targeted nano-liposome and application thereof, and the B cell or CD11b + cell targeted nano-liposome is prepared from polyethylene glycol and derivatives thereof, cholesterol, phosphate fat and derivatives thereof which are self-assembled in different proportions and selectively act on B cells or CD11b + cells in a targeted manner under the condition that bioactive molecules are not coupled. And various anti-cancer new dosage forms, vaccine dosage forms and gene therapy vectors are prepared based on the nano-liposome capable of targeting B cells or CD11b + cells.

The invention discloses a synthesis method of a polysubstituted cyclopropyl carbonyl derivative, and belongs to the technical field of organic synthesis and the technical field of medicine synthesis. The method comprises the following steps: (1) taking substituted olefin as a raw material, and obtaining alpha-chlorocyclobutanone through [2 + 2] cycloaddition and reduction reaction; and (2) carrying out rearrangement reaction on the alpha-chlorocyclobutanone and different types of Grignard reagents or organic lithium reagents to obtain the polysubstituted cyclopropyl carbonyl derivative. The synthesis method provided by the invention has the advantages of wide substrate range, good functional group compatibility, mild reaction conditions, no need of preparation of active intermediates or use of expensive transition metal catalysts, simple operation, capability of obtaining various types of cyclopropyl carbonyl compounds, and the like. The practicability of the method is further shown through later-stage functional group modification of complex bioactive molecules and abundant derivatization of polysubstituted cyclopropyl carbonyl products of the complex bioactive molecules.

Disclosed are formulations for providing an active agent. Formulations include a carrier including an active agent and mineral coated microparticles wherein an active agent is adsorbed to the mineral. Other formulations include a carrier including mineral coated microparticles wherein mineral coated microparticles include an active agent. Also disclosed are methods for sustained delivery of an active agent and methods for treating inflammatory diseases using a formulation for providing sustained delivery of an active agent.

Methods for achieving controlled and sustained active release of biologically active molecules and their applications in medicines. [Solution] Protein or peptide drugs have problems such as short half-life, large fluctuations in blood concentration, and low safety. In particular, direct administration of IL-2 and other drugs has significant toxicity and side effects, limiting their clinical application. Conventional techniques attempt to solve the above problems by PEG modification, but the activity of drugs after PEG modification decreases, and active release and bioavailability are poor. The present invention achieves active release control and sustained release of bioactive molecules using a specific PEG modifier. In particular, the complex of the PEG modifier and IL-2 gradually releases the activity of IL-2 as the PEG is removed, achieving a dynamic balance of excellent bioavailability and stable effective blood concentration, and is expected to have benefits in clinical application such as reduced administration frequency, improved drug bioavailability, patient compliance, and safety.

This invention relates to compositions, and uses and methods thereof, with therapeutic deciparticles. Described herein are deciparticle (nanoparticle) compositions composed of an amphiphilic compound complexed with an auxiliary compound such as a biologically active molecule. Deciparticles of this invention are active drugs having potency for anti-tumor effects and for immunosuppression. This invention is also directed to amphiphilic compounds useful for making deciparticle complexes.

Therapeutic combinations, pharmaceutical compositions, and pharmaceutical kits are provided, comprising fungi (e.g., Psilocybe spp.), plants (e.g., Cannabis spp., Dipteryx spp.), and algae (e.g., from the family Bangiaceae, including Pyropia spp. and Porphyra spp.), including extracts thereof and bioactive molecules derived therefrom. Also provided are methods for producing the combinations, compositions, and kits such as through natural, biosynthetic, or synthetic means. Further provided are methods of use for treating medical conditions, particularly mitochondrial and other disorders, wherein the disclosed combinations and compositions exhibit synergistic effects and therapeutic and other advantages.

The invention relates to a spider neurotoxin tail peptide with a cell transmembrane function and application of the spider neurotoxin tail peptide. The amino acid sequence of the spider neurotoxin tail peptide with the cell penetrating function is as shown in SEQ ID NO: 2. The invention also provides application of the cell-penetrating peptide in preparation of a carrier which is used for delivering bioactive molecules and can penetrate cell membranes. The invention further provides a fusion protein composed of the spider neurotoxin tail peptide and spider neurotoxin omega-Pp1b and application of the fusion protein in preparation of insecticides. The invention also provides an amphiphilic peptide and application thereof in preparation of a carrier which is used for delivering bioactive molecules and can penetrate through a cell membrane. The invention also provides a nano-composite and application of the nano-composite in preparation of a preparation for insect cell gene silencing. The invention also provides a pesticide composition. The invention is a novel cell-penetrating peptide derived from an insect system, and has important significance for promoting the development of peptide biological insecticides and RNA pesticides.

The application belongs to the technical field of biological medicine and molecular biology, and particularly relates to application of umbilical cord blood plasma-derived extracellular vesicles and related bioactive molecules thereof in treatment of Alzheimer's disease. Specifically, the application isolates extracellular vesicles (UCBP-sEVs) from umbilical cord blood plasma, which has the effect of improving Alzheimer's disease. Further research finds that high enrichment of miR-16-2-3p therein is a key molecule for mediating treatment of Alzheimer's disease. miR-16-2-3p targets and inhibits expression of ROCK2, reduces phosphorylation level of TFEB and promotes nuclear translocation of the same, activates microglial autophagy-lysosome pathway, and thus promotes phagocytosis and degradation of intracerebral beta amyloid, and therefore has good practical application value.

The invention relates to an aromatic ester substituted nitrogen-containing heterocyclic compound and a preparation method and application thereof.The preparation method comprises the steps that a heterocyclic compound, aldehyde and an oxidizing agent are dissolved in a solvent and stirred for several hours at the room temperature under blue light irradiation and nitrogen protection, and after the reaction is finished, the ester nitrogen-containing heterocyclic compound is obtained through aftertreatment. The method is mild in reaction condition, simple, convenient and safe to operate and cheap and easily available in raw materials, is an environment-friendly green synthesis method, can be successfully applied to synthesis of potential drug molecules with anti-tumor activity, and provides a convenient means for bioactive molecules and drugs.

Disclosed are formulations for providing an active agent. Formulations include a carrier including an active agent and mineral coated microparticles wherein an active agent is adsorbed to the mineral. Other formulations include a carrier including mineral coated microparticles wherein mineral coated microparticles include an active agent. Also disclosed are methods for sustained delivery of an active agent and methods for treating inflammatory diseases using a formulation for providing sustained delivery of an active agent.

The invention discloses a method for synthesizing chiral morpholine from propargyl alcohol ester. Chiral morpholine is an important drug molecular skeleton and is widely applied to the aspects of analgesia, anesthesia, tumor resistance, heart treatment and the like as a drug active ingredient, but an efficient synthesis method is lacked. According to the method disclosed by the invention, under the regulation and control of arylboronic acid and a specific chiral ligand, propargyl alcohol ester and an affinity reagent react to obtain optically pure (87-97% ee) morpholine. The method has the characteristics that the catalyst and the ligand are wide in source, and the substrate is cheap and easy to obtain; the chiral morpholine has excellent enantioselectivity and good functional group compatibility, can be suitable for structural modification of bioactive molecules and intermediates, and is a simple and efficient asymmetric catalysis strategy for synthesizing chiral morpholine.

The invention provides an imino methyl phosphine reagent and application thereof in preparation of cyclopropylamine compounds, and belongs to the technical field of organic chemistry. A method for preparing a cyclopropylamine compound from the imino methyl phosphine reagent comprises the following steps: dissolving the phosphine reagent in an organic solvent, cooling to a certain temperature, adding alkali, stirring, adding an epoxy compound, heating to a certain temperature, reacting, carrying out acidolysis to obtain cyclopropylamine salt, and carrying out alkali neutralization to obtain free cyclopropylamine. According to the imino methylphosphine reagent and the application thereof in preparation of cyclopropylamine compounds, a target product is synthesized in one step from epoxy compounds, the defects that a traditional method is tedious in step, toxic reagents are used, the yield is low and the like are overcome, the synthesis efficiency and the yield are improved, the use of harmful reagents and organic solvents is reduced, and the cost is reduced. And primary free cyclopropylamine is easy to obtain and is convenient to subsequently convert into medicines and bioactive molecules.

The present disclosure relates to extracellular vesicles (e.g., exosomes) comprising a biologically active molecule covalently linked to the extracellular vesicle via a dual cleavable linker and an anchoring moiety. The extracellular vesicles can be useful as an agent for the prophylaxis or treatment of cancer or other diseases. Also provided herein are methods for producing the extracellular vesicles and methods for using the extracellular vesicles to treat diseases or disorders.

The invention is directed to fertilizers and manufacturing methods using organically enhanced inorganic fertilizer granules that incorporate a coating of one or more layers containing a bioactive agent in a carrier. The bioactive agent may be an herbicide, pesticide, plant growth regulator, microorganism, or beneficial element. Manufacture of conventional fertilizers involves stresses such as pH, heat, and pressure that are overcome by providing a protective carrier that facilitates and extends functional survival / effectiveness. Many carriers, such as liquefied dried milk, bind actively to the granule surface and contribute to the total carbon base. The release of the bioactive agent from the coating and or the surface of the fertilizer granule preferably results in a two-phased release, a first fast release and a second extended or slow-release into the soil metering the bioavailability of the bioactive agent for crop growth or protection, and / or for controlling unwanted vegetation or pests.

The present invention is in the field of biomedicine and drug delivery as well as pest and vector control. The present invention relates to a novel family of silicon-introduced ionizable cationic lipids belonging to the trademark LipexSill second generation lipids wherein the tail is linked to the head group via a biodegradable silicon-based acetal linker. Lipids containing a silicon-based acetal linker are the most advanced, and are effective as ionizable cationic lipids in formulating empty or loaded lipid nanoparticles (LNPs). The novel linker according to the present invention is [WO2022129966] designed using a proprietary borane catalyst. The present invention describes the synthesis of lipids of formula (I), the formation and characterization of nanoparticles, and biological experiments that prove that lipid nanoparticles prepared with these novel lipids can effectively deliver their cargo receptors (cargo) (e.g., RNA, DNA, mRNA, siRNA, dsRNA, pDNA, microRNA, circular DNA, small bioactive molecules) into cells.

The application belongs to the technical field of organic synthesis, and particularly relates to a kind of bromine-containing isoindoline-1-ketone compound and preparation method thereof.The preparation method of the bromine-containing isoindoline-1-ketone compound uses commercially available aldehyde-derived imine as raw material, is reacted with aryl bromide oxazoline compound under butyl lithium condition, and then is subjected to acid-mediated cascade cyclization process, to efficiently construct isoindoline-1-ketone skeleton.The isoindoline-1-ketone compound can be directly used as an organic catalyst, the N-H functional group remaining in the structure of the isoindoline-1-ketone compound has reactivity, can be coupled with other bioactive molecules as a key connection site, to construct functional derivatives, the amide carbonyl group thereof can be further reduced, to be converted into pyrrolidine structural unit, and the structure itself can be used as a catalytically active center, to expand its application in the field of catalysis.

The invention provides an S-adenosine homocysteine (SAH) analogue, an S-adenosine-L-methionine (SAM) analogue and application thereof. The preparation method comprises the following steps: synthesis of the SAH analogue and a fluoroalkyl SAM analogue, fluoromethylation modification of bioactive molecules by an HMT-MT cyclase cascade reaction system based on the fluoroalkyl SAM analogue, and construction of a fluoro derivative of a clinical drug synthesized by a one-pot enzymatic method. The SAH analogue adopted by the invention can effectively avoid spontaneous degradation of the corresponding SAM analogue, and is used for constructing a cascade reaction system based on HMT-MT cyclase, so that the yield of a fluoromethylation product is increased; it is confirmed that the fluoro-intermediate generated by MT can be accepted by downstream biosynthetase, so that a fluoro-derivative of a clinical drug synthesized by a one-pot enzymic method is constructed.

The invention relates to a method, expression system and related kit for producing at least one biologically active molecule, in particular a biotherapeutic, by optogenetic control of gene expression in at least one eukaryotic or prokaryotic cell, wherein the biologically active molecule comprises at least one protein of interest comprising at least two different subunits. In particular, one embodiment of the expression system according to the invention comprises three expression cassettes (2, 3, 4) for optogenetic control of the production of a protein of interest comprising two subunits (5, 6). A first expression cassette (2) comprises a first nucleic acid sequence (7) that is operably linked to a first promoter (8) and encodes a photosensitive transcription factor (9) comprising a gene expression controlling domain (10). The expression system (1) further comprises a second expression cassette (3) comprising a second nucleic acid sequence (11) encoding the first subunit (5) of the protein of interest. The second nucleic acid sequence (11) is operably linked to a second promoter (12) being operably linked to a transcription factor binding site (13) designed to bind the photosensitive transcription factor (9). The expression system (1) also comprises a third expression cassette (4) comprising a third nucleic acid sequence (15) encoding the second subunit (6) of the protein of interest and being operably linked to a third promoter (16).

The invention discloses a method for synthesizing an amino-selenium nitrogen heterocyclic compound through near-infrared light catalysis, according to the method, the amino-selenium nitrogen heterocyclic compound is efficiently synthesized through catalysis of a near-infrared light response type anthraquinone polymer, efficient coupling of an unprotected amino group and a selenium nitrogen heterocyclic ring is successfully achieved, the reaction process is accurately regulated and controlled through photocatalysis, and the yield of the amino-selenium nitrogen heterocyclic compound is improved. The construction of a series of amino-selenium nitrogen heterocyclic compounds is completed under mild conditions. According to the method, the natural reaction activity of amino is reserved, the electronic structure of a heterocyclic skeleton is optimized through the electronic effect of selenium atoms, and a green and sustainable technical solution is provided for functional modification of selenium-containing bioactive molecules.

The invention discloses a method for synthesizing functional pyrrole through photocatalysis of N-arylglycine and 1, 3-eneyne. According to the method, N-arylglycine is decarboxylated through photocatalysis to form an alpha-amino alkyl free radical, and the free radical and 1, 3-eneyne are subjected to free radical addition, cyclization and oxidative aromatization reaction to construct polysubstituted pyrrole. Pyrrole serves as a heterocyclic compound with great importance, widely exists in numerous drug compounds and bioactive molecules, shows electronic characteristics with great prospects in organic photovoltaic devices (OPVs) and organic field effect transistors (OFETs), is also a key structural unit in synthesis of pesticides, natural products and dyes, and has a broad application prospect. Powerful support is provided for multi-industry development, and the application prospect is wide. The polysubstituted pyrrole compound is synthesized through a one-pot method, and a new method is provided for preparing the novel polysubstituted pyrrole compound.

Disclosed is a method for producing biocrude and bioactive substances from microalgae biomass. The method has the steps of mixing and stirring dry microalgae biomass with water and an acid catalyst, heating the mixture at high pressure at a temperature and time based on each individual species or processing the biomass mixture in a colloidal mill with solvent, separating lysed algae cells into non-polar extracts from water-soluble extracts via vacuum filtration, washing the lysed algae cells and non-polar extracts with organic solvents, separating the organic solvent mixture, which has ethanol and long-chain fatty acids, from the remaining biochar via vacuum filtration, and separating the ethanol from the fatty acids via distillation or rotary evaporator to extract bio-oil.