227 results about "Bioactive molecules" patented technology

The invention provides a stem cell exosome vesicle induced by traditional Chinese medicine functional components as well as a preparation method and application thereof, and belongs to the technical field of biological medicines. According to the preparation method of the stem cell exosome vesicle, traditional Chinese medicine functional components serve as an exosome inducer, stem cells can be induced to proliferate and secrete exosome with the enhanced function, the yield of the exosome can be increased, bioactive molecules can be loaded, and the bioavailability of the exosome in diabetes treatment is remarkably improved. The stem cell exosome vesicle disclosed by the invention can be applied to treatment of diabetes and complications thereof, not only can improve functions of islet cells, but also can treat chronic inflammation, microangiopathy and other metabolic diseases related to diabetes, and has a wide clinical application prospect.

The invention relates to an antibody drug conjugate which is shown in a formula (I) and contains two or more bioactive molecules with different action mechanisms, a preparation method of the antibody drug conjugate, and application of the antibody drug conjugate in prevention and / or treatment of diseases related to abnormal cell activity, including but not limited to prevention and / or treatment of tumor diseases. # imgabs0 #

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.

The invention discloses a synthesis method of a novel benzosuberone compound, and belongs to the field of organic synthesis. The preparation method comprises the following steps: uniformly stirring methyltriphenylphosphonium bromide in a solvent at room temperature, dropwise adding an n-hexane solution of n-butyllithium in an ice-water bath, stirring a reaction system at room temperature for 30-40 minutes after dropwise adding is completed, then adding an initial raw material phenanthrenequinone 1 in the ice-water bath, transferring the reaction system to 40 DEG C for reaction, and after the reaction is monitored to be complete by a TLC (Thin Layer Chromatography) dot plate, filtering, washing and drying to obtain the phenanthrenequinone 1. And pouring the reaction liquid into a silica gel chromatographic column, and simply filtering by using dichloromethane as an eluent to remove salt and phosphine oxide. And performing rotary evaporation to remove the organic solvent to obtain a crude product, and separating and purifying to obtain a target product 2. The method is short in reaction time and low in reaction cost, provides a practical method for obtaining the seven-membered rigid ring skeleton, and has potential value for synthesis of natural products and bioactive molecules.

The present disclosure relates to novel lipids for delivering one or more biologically active molecules to a subject. The present application also relates to a composition or a nanoparticle comprising said lipid, methods of preparing said lipid, use of said lipid and method of using said lipid.

The invention provides a spiro butane indolone derivative as well as a preparation method and application thereof, and belongs to the technical field of organic chemical synthesis. The series cyclization coupling reaction of the N-iodo aryl dicyclobutyl amide compound and the vinyl pyridine compound is realized by utilizing a photocatalytic system, and the method is used for constructing the spiro butane indolone derivative containing the pyridine structure. The spirobutane indolone derivative synthesized by the invention has an inhibition effect on H1975 human lung adenocarcinoma cells; the preparation method provided by the invention is mild in condition and simple and convenient to operate, has economical steps, provides a convenient synthesis way for the complex bioactive molecules, and has a good application prospect.

The invention provides a membrane-wrapped organelle-like system for directionally assembling membrane protein, which comprises a molecular framework and a closed lipid bilayer membrane wrapping the outer side of the molecular framework, the molecular framework is loaded with load molecules, the molecular framework directionally recombines the lipid bilayer membrane through a transmembrane region of the membrane protein, and the lipid bilayer membrane is loaded with the load molecules. The lipid bilayer membrane provides a barrier and protection for a molecular framework and loaded molecules, and the lipid bilayer membrane is provided with directional recognition molecules. According to the invention, a molecular framework wrapped by a lipid bilayer membrane is utilized, and a novel technology capable of simulating lipid vesicles of an organelle membrane framework is adopted, so that a brand-new directional delivery function on specific cells or specific organelles in the specific cells can be endowed. And oriented assembly of a membrane protein compound and effective loading of bioactive molecules are realized by using a process of chemically recombining the lipid bilayer membrane.

The present disclosure provides compositions and methods of recovering a policosanol or a sterol from a mixture comprising one or more fatty alcohols, aldehydes, fatty acids, and / or sterols. The mixture may be, for example, a lipid extract obtained from industrial fermentation processes (e.g., filter cake, distillate residue). The policosanol and / or sterol fraction recovered may be enriched in certain fatty alcohols (e.g., 1-octacosanol, 1-triacontanol, and / or 1-dotriacontanol), or enriched in certain sterols (e.g., ergosterol, campesterol, stigmasterol, and / or β-sitosterol). These bioactive molecules may be useful in the treatment or prevention of various metabolic conditions (e.g., obesity, dyslipidemia, cardiovascular conditions, and other chronic metabolic diseases).

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.

The invention belongs to the technical field of biomedical materials, and discloses microgel assembly powder capable of rapidly stopping bleeding as well as a preparation method and application of the microgel assembly powder. The microgel assembly powder is composed of microgel powder and assembly agent powder, and the mass ratio of the microgel powder to the assembly agent powder is (1: 10)-(10: 1); the microgel powder comprises carboxymethylated and sodium trimetaphosphate cross-linked dual-modified polymer powder, and the assembling agent powder is polyphenol modified polymer powder. The microgel assembly powder can quickly absorb moisture in blood to concentrate the blood after being in contact with the blood, meanwhile, rich ortho-phenolic hydroxyl groups on the assembly agent can immediately form a hydrogen bond network among microgel, red blood cells and platelets, and the microgel assembly powder is assembled into hydrogel with excellent mechanical strength and adhesion performance. In addition, the powder can load bioactive molecule thrombin, activate multiple blood coagulation cascade reaction and promote formation of a fibrous protein network and blood clots, and through the synergistic effect of multiple hemostasis mechanisms, the powder shows rapid and effective hemostasis performance.

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.

The invention relates to the technical field of degradable materials, in particular to a preparation method of an amino acid-based degradable material, which comprises the following steps: S1.1, converting calcium glutamate into an amidate under the catalytic action; s1.2, mixing the amidate with threonine phosphate to prepare a sediment; s1.3, the sediment is further modified with citric acid, and a degradable base material is obtained; and S1.4, fully and uniformly mixing the degradable base material, the bioactive molecules, the plasticizer, the stabilizer and the antioxidant, and performing extrusion molding by using a double-screw extruder to obtain the amino acid-based degradable material. Wherein the degradable base material is prepared from calcium glutamate, threonine phosphate and citric acid according to the mass ratio of 7: (3-4): (0.5-1); the calcium glutamate is adopted to construct a material basic framework, the phosphothreonine further enhances the structural stability and improves the mechanical strength, the mechanical performance and the degradation period are balanced, and wide application prospects are achieved.

The invention discloses a sulfur-containing gem-difluoroallyl compound as well as a preparation method and application thereof. The invention provides a preparation method of a compound as shown in a formula C. The preparation method comprises the following step: in a solvent, in the presence of alkali, carrying out gem-difluoroallylation reaction on a compound as shown in a formula A and a compound as shown in a formula B to obtain the compound as shown in the formula C. According to the method, the sulfydryl in the sulfydryl-containing compound can be mildly and efficiently gem-difluoroallylated, metal catalysis is not needed, the reaction can be performed in a water phase, the operation is simple, and the method is suitable for performing rapid fluoroalkylation modification and further functional modification on polypeptide, protein, complex bioactive molecules and the like; the method has very important application prospects in the fields of medicine, life science and the like.

The present invention proposes a kind of synthetic method of 2 thiobenzothiazole compounds, with 2 iodinated aryl isothiocyanates and thiol as substrates, add alkali (potassium carbonate) and catalyst / ligand (cuprous iodide / 1,10 phenanthroline) reaction, 2 thiobenzothiazole compounds can be efficiently synthesized. Compared with prior art, this method has fast reaction rate and conversion rate close to quantitative; Reaction conditions are mild, green and friendly and post-processing is simple; Substrate has a wide range of applications, and rich structural target objects can be obtained; Method is simple and easy, does not require inert gas protection, and is insensitive to air moisture. 2 thiobenzothiazole compounds are important skeletons of many drugs and bioactive molecules, and this method can provide a widely applicable preparation method for the synthesis of such compounds.

The present disclosure relates to extracellular vesicles (e.g., exosomes) comprising a bioactive molecule covalently linked to the extracellular vesicles via a cleavable linker and an anchoring moiety, the cleavable linker comprising a cell penetrating peptide. The extracellular vesicles can be used as agents for the prevention or treatment of cancer or other diseases. Also provided herein are methods for producing the extracellular vesicles and methods for treating a disease or condition using the extracellular vesicles.

The invention relates to an antibody drug conjugate for treating tumors, and belongs to the technical field of biological medicines. The invention provides an antibody drug conjugate for treating tumors. The structural general formula of the antibody drug conjugate is Ab-[L1-L2-L3-L4-D] p, wherein Ab is a monoclonal antibody targeting a tumor cell surface antigen, D is a bioactive molecule having an inhibition effect on tumor cells, p is drug loading capacity, and L1-L2-L3-L4 are linkers connecting the monoclonal antibody and the bioactive molecule. The antibody drug conjugate has good druggability. Meanwhile, the antibody drug conjugate has an obvious in-vitro cell killing effect on NCI-H82 cells, SHP-77 cells and DMS-53 cells, and the antibody drug conjugate can obviously reduce the volume of tumors in NCI-H82 tumor-bearing mice and SHP-77 tumor-bearing mice and has a great application prospect in tumor treatment.

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.

The invention belongs to the technical field of synthetic chemistry, and particularly relates to a synthetic method of trisubstituted phosphine and oxygen / sulfur / boride thereof. According to the method, halogenated hydrocarbon and a diaryl / alkyl phosphine compound are taken as reaction substrates, the trisubstituted phosphine is prepared through direct one-step reaction without any other catalyst, additive or solvent, and the oxygen / sulfur / boride of the trisubstituted phosphine is obtained through further simple conversion. The synthesis method disclosed by the invention is green and environment-friendly, efficient in reaction, cheap and easily available in raw materials, simple to operate, good in atom economy, good in substrate applicability and high in yield. The efficiently synthesized trisubstituted phosphine and the oxygen / sulfur / boride thereof are important skeletons of many drugs, bioactive molecules and natural products. The synthesis method provided by the invention provides a widely applicable preparation method for synthesis of the compounds.

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.