91 results about "Enzyme inhibitory" patented technology

The invention discloses a xanthine oxidase inhibitory peptide with uric acid reducing activity and application thereof, and belongs to the technical field of biological medicines.The xanthine oxidase inhibitory peptide is obtained by conducting enzymolysis, separation and purification on processing byproducts such as litopenaeus vannamei heads and shells with xanthine oxidase inhibitory activity. The xanthine oxidase inhibitory peptide is screened by using a molecular docking technology, and the amino acid sequence of the xanthine oxidase inhibitory peptide is Pro-Pro-Val-Pro-Pro-Pro. The xanthine oxidase inhibitory peptide has an XOD (X-Oxidase) half inhibitory concentration of 3.181 + / -0.1786 mM. The invention further proves that the xanthine oxidase inhibitory peptide has a certain improvement effect on hyperuricemia mice, and the xanthine oxidase inhibitory peptide mainly has the effects of reducing the content of serum uric acid, creatinine and urea nitrogen of the hyperuricemia mice, inhibiting the activity of xanthine oxidase (XOD) in serum and liver of the mice, inhibiting synthesis of uric acid and improving kidney injury of the mice, and the xanthine oxidase inhibitory peptide has a certain improvement effect on the hyperuricemia mice through Toxinpred prediction. The xanthine oxidase inhibitory peptide uric acid reducing peptide is free of toxic and side effects and has a wide market application prospect.

The invention discloses a hexapeptide TE6 with xanthine oxidase inhibitory activity and a preparation method and application thereof, and belongs to the technical field of small molecule peptides. The amino acid sequence of the hexapeptide TE6 is TIATVE, and the hexapeptide TE6 can be prepared through a solid-phase synthesis method and an enzymolysis method. The hexapeptide TE6 is identified from a solieria cavaleriei proteolysis solution and has potential interaction with xanthine oxidase, under the concentration of 0.1 mg / mL, the xanthine oxidase inhibition rate is 44.74%, and compared with goose carnosine (the xanthine oxidase inhibition rate is 36.03%), the xanthine oxidase inhibition rate is remarkably increased (plt; 0.05), which is stronger in xanthine oxidase inhibitory activity, and can be used for preparing a preparation for inhibiting xanthine oxidase activity and relieving hyperuricemia.

The invention discloses spirulina protein-zein composite nanoparticles and a preparation method and application thereof.The preparation method comprises the steps that a zein solution is added into a spirulina protein solution, ethanol in the solution is removed through evaporation, insoluble substances are removed through centrifugation, and spirulina protein-zein composite nanoparticle dispersion liquid is obtained; and freeze-drying to obtain spirulina protein-zein composite nanoparticle powder. The preparation method of the spirulina protein-zein composite nano-particles is simple, low in cost, green and safe, and the obtained nano-particles can be kept stable in a neutral pH environment, have good biocompatibility, can be applied to efficient embedding of bioactive components, and have good application prospects. The light, heat and storage stability of the bioactive components are remarkably improved; and the oxidation resistance, tyrosinase inhibition and in-vitro release performance of the bioactive components are improved.

The invention discloses a procyanidine trimer compound, which has a chemical structure as shown in the specification. The hypoglycemic potential of the compound is evaluated through an in-vitro enzyme inhibition experiment, and the result shows that the compound has a remarkable inhibition effect on alpha-amylase, has good water solubility, is derived from natural plant resources, is clear in structure and good in safety, and has a huge application prospect in development of novel natural-source hypoglycemic drugs.

Provided are an amphotericin B amide derivative and a use thereof. The amphotericin B amide derivative is as shown in formula (I). The compound has good antifungal activity, is effective against various fungi, has good water solubility, is adapted to be developed into an injection dosage form, has excellent metabolic stability in animals (such as mice, rats, dogs, and monkeys), has a long half-life period, can effectively reduce the frequency of administration, has weak inhibition on CYP enzymes, and has a low risk of drug interaction.

The invention provides an amphotericin B amide derivative and application thereof. The amphotericin B amide derivative is shown as a formula (I), has good antifungal activity, is effective to various fungi, has good water solubility, is suitable for being developed into injections, has excellent metabolic stability in animal bodies (such as mice, rats, dogs and monkeys), is long in half-life period, can effectively reduce the administration frequency, is weak in CYP enzyme inhibition, and can be used for preparing the antifungal drugs. The drug interaction risk is low.

The invention discloses high-safety and high-activity chickpea fermentation liquor as well as a preparation method and application thereof. The fermentation liquor is prepared by fermenting chickpeas through specific kefir grain symbiotic flora, the phytic acid content in the raw materials is remarkably reduced to be smaller than or equal to 0.4%, the oxalic acid content is remarkably reduced to be smaller than or equal to 0.07%, the phytic acid content and the oxalic acid content are far lower than those of a water extraction method, an enzymolysis method and a single-strain fermentation method, and potential damage of anti-nutritional factors to scalp is effectively eliminated. Meanwhile, rich active ingredients such as chickpea essence A, small molecular protein peptide and kefir grain lysate are generated in the fermentation process. Experiments show that the fermentation liquor can efficiently inhibit 5alpha-reductase (the inhibition rate is larger than or equal to 80%) and remarkably promote regeneration of mouse hair follicles, has excellent oxidation resistance and malassezia activity inhibition, and can be used for preparing hair products for preventing hair loss and maintaining hair follicles.

This invention discloses the preparation and application of a substituted heteroaryl ketone compound. The structure of the substituted heteroaryl ketone compound is shown in Formula I, wherein the definitions of each substituent are as described in the specification and claims. The compound of this invention has MAT2A enzyme inhibitory activity and, as a MAT2A inhibitor, can be used to prepare drugs for treating or preventing diseases of MAT2A overexpression and diseases of gene deletion encoding methionine phosphorylase.

The invention relates to the technical field of medicines, in particular to a novel triterpenoid glycoside compound extracted from rosa roxburghii tratt fruits and a preparation method and application of the novel triterpenoid glycoside compound. The novel triterpenoid glycoside compound is Roxbuterene E, the molecular formula of the novel triterpenoid glycoside compound is C41H66O13, the novel triterpenoid glycoside compound is obtained by separating and purifying a rosa roxburghii tratt fruit methanol extract by adopting normal-phase silica gel column chromatography, reversed-phase ODS column chromatography and HPLC (High Performance Liquid Chromatography), and a PTP1B enzyme inhibitory activity experiment proves that the novel triterpenoid glycoside compound has potential activity for treating diabetes. And technical support is provided for research and development of novel diabetes treatment drugs.

Disclosed in the present invention are a PARP1 / CDK6 dual-target inhibitor, and a preparation method therefor and the use thereof. The PARP1 / CDK6 dual-target inhibitor is a compound having a structure represented by formula I, or a pharmaceutically acceptable salt or solvate thereof, wherein L is selected from or , and R is selected from the group consisting of hydrogen, deuterium, halogen, hydroxyl, sulfhydryl, cyano, nitro, methoxy, a C1-C8 alkyl, or a C3-C8 cycloalkyl. The PARP1 / CDK6 dual-target inhibitor of the present invention exhibits good effects against human breast cancer cells, and maintains a good in vitro enzyme inhibitory activity against CDK6 and PARP1. Disclosed in the present invention is the use of a CDK6 / BRD4 dual-target inhibitor in the preparation of a drug for treating PARP1 / CDK6-mediated diseases. Disclosed in the present invention is the use of a PARP1 / CDK6 dual-target inhibitor in the preparation of a drug for treating or preventing triple-negative breast cancer.

The invention belongs to the technical field of biological medicines and bioactive peptides, and relates to a xanthine oxidase inhibitory peptide derived from goat milk protein and application thereof. The amino acid sequence of the xanthine oxidase inhibitory peptide is as shown in SEQ ID NO. 1. The xanthine oxidase inhibitory peptide can be used for preparing a product for inhibiting xanthine oxidase or a product for regulating and controlling the uric acid level in a human body. The XOD regulation active peptide provided by the invention is safe in source and clear in structure, can be applied to the field of functional food or nutrition intervention, and provides a safe and natural active substance basis for diet regulation of hyperuricemia and related metabolic diseases.

A compound exhibiting coronavirus 3CL protease inhibitory activity or a pharmaceutically acceptable salt thereof, represented by Formula (I)wherein Ring A is a ring represented by:wherein X is a single bond or the like, R2 is substituted or unsubstituted aromatic carbocyclyl or the like, R3c is substituted or unsubstituted aromatic carbocyclyl or the like, R3 is substituted or unsubstituted aromatic carbocyclyl or the like, R3a is a hydrogen atom or the like, R3b is a hydrogen atom, R8a is substituted or unsubstituted aromatic carbocyclyl or the like, and R8b is a hydrogen atom or the like,R1 is a substituted or unsubstituted aromatic heterocyclyl, m is 0 or the like, R5a is each independently a hydrogen atom or the like, R5b is each independently a hydrogen atom or the like, R6 is cyano or the like, and R7a and R7b are each independently a hydrogen atom or the like.

The application relates to the technical field of biological medicine, in particular to a compound with a conjugated structure containing an alpha, beta-unsaturated aldehyde and application thereof. The compound can covalently modify Sortase A enzyme of propionibacterium acnes through alpha, beta-unsaturated aldehyde, inhibit transpeptidation catalysis and adhesion of gram-positive bacteria (for example, methicillin-resistant staphylococcus aureus, streptococcus mutans and propionibacterium acnes), block anchoring of membrane proteins, inhibit growth of gram-positive bacteria or kill bacteria; conjugated groups with different electric effects and steric effects are screened to adjust the covalent modification efficiency of alpha, beta-unsaturated aldehyde and Sortase A enzyme, strengthen the activity of the compound in inhibiting Sortase A enzyme, thereby improve the antibacterial activity of the compound, and further make the compound with the conjugated structure containing the alpha, beta-unsaturated aldehyde in the application be applied to the fields of biological medicine and cosmetics as an antibacterial component.

The present invention provides industrially suitable processes for preparing intermediates in the production of substituted polycyclic pyridone derivatives having a cap-dependent endonuclease inhibitory activity. In the process as shown below, wherein each symbol is as defined in the specification, an optically active substituted tricyclic pyridone derivative of the formula (VII) is obtained in high yield and high enantioselectivity by subjecting a compound of the formula (III) or (VI) to intramolecular cyclization with controlling stereochemistry to obtain a compound of the formula (IV) having a removable functional group on an asymmetric carbon, and then removing the functional group thereof;

The invention discloses a multifunctional fermented soya bean polypeptide and application thereof, and relates to the field of food processing technologies and seasoning base materials. According to the invention, the multifunctional fermented soybean polypeptide (FGDEL) is obtained through screening. According to tests on oxidation resistance, Fe < 3 + > reduction capacity and tyrosinase inhibition capacity, the multifunctional fermented soya bean polypeptide has certain oxidation resistance, Fe < 3 + > reduction capacity and tyrosinase inhibition capacity, so that technical support is provided for developing oxidation-resistant products, products for improving iron-deficiency anemia (helping to improve iron element absorption) and whitening products.

The application belongs to the technical field of microorganisms, and discloses a bacillus amyloliquefaciens D189 with high yield of extracellular polysaccharide. The bacillus amyloliquefaciens D189 is preserved in China Center for Type Culture Collection on April 29, 2021, and the preservation number is CCTCC NO: M2021484. The bacillus amyloliquefaciens D189 provided in the application has high yield of extracellular polysaccharide, the yield of the crude extracellular polysaccharide EPS-OD is 131.31+ / -2.13 g / L after optimization, the extracellular polysaccharide EPS is obtained by purifying the crude EPS-OD through a DEAE ion exchange column, and the composition of the crude EPS-OD and the EPS is determined. The extracellular polysaccharide of the bacillus amyloliquefaciens D189 has good alpha-glucosidase inhibitory capacity and pancreatic lipase inhibitory capacity, and good total bile acid and cholesterol micelle binding capacity in vitro, so that the extracellular polysaccharide and the lipid-lowering and glucose-lowering product have good application prospects.

This invention discloses a crayfish head protein peptide with uric acid-lowering effect and its application, belonging to the field of biotechnology. The amino acid sequence of the crayfish head protein peptide is shown in any one of SEQ ID NO. 1-4. This invention uses ultrasonic and microwave technology to assist protein hydrolysis, prepares xanthine oxidase inhibitory peptides from crayfish heads, explores the material basis of its activity, and studies its mechanism of action, laying a theoretical foundation for the high-value utilization of crayfish processing by-products and the development of food-derived xanthine oxidase inhibitors.

The invention belongs to the technical field of biological medicine, and particularly relates to an alpha-amylase inhibitory active peptide and application thereof.The alpha-amylase inhibitory active peptide is separated from free peptide of smelly mandarin fish, and the amino acid sequence of the alpha-amylase inhibitory active peptide is shown as any one of Leuu-Pro-Lys-Leu-Arg-Val-Lys-Val; val-Glu-Lys-Ser-Lys-Val-Tyr is selected from the group consisting of Glu-Lys-Ser- Glu-Val-Ile-Glu-Leu-Asp-Trp-Arg is selected from the group consisting of Glu-Val-Ile-Glu- The active peptide has good alpha-amylase inhibitory activity, and can be applied to preparation of an alpha-amylase inhibitor, a hypoglycemic drug or a drug for preventing or treating hyperglycemia-related diseases.

The invention relates to a CDK12 / PARP double-target inhibitor and a preparation method and application thereof, the structural general formula (I) of the inhibitor is shown in the specification, in particular to the CDK12 / PARP double-target inhibitor and the preparation method and application thereof, pharmacodynamic tests prove that the CDK12 / PARP double-target inhibitor has a remarkable anti-tumor effect, and the CDK12 / PARP double-target inhibitor has a good application prospect. The CDK12 / PARP double-target inhibitor comprises a substituted compound with a general formula (I), or a stereoisomer, a hydrate or a pharmaceutically acceptable salt thereof. Compared with the prior art, the compound is novel in structure, and experiments show that the compound has good CDK12 and PARP enzyme inhibitory activity and can be used for preparing CDK12 / PARP double-target antitumor activity drugs.

According to the method for fermenting the traditional rare Chinese herbal medicine in the duplex tank reactor through the saccharomycetes, fermentation is conducted through the Saccharomyces cerevisiae YALAN1, the content of effective substances in a fermentation product is increased, and it is guaranteed that the fermentation product has certain oxidation resistance and tyrosinase inhibitory activity; and the fermentation process is carried out in the duplex tank reactor, so that the small-scale test fermentation level in a laboratory is successfully improved to the pilot-scale test fermentation level (5L * 2), and the method has guiding significance for industrial application. In the whole fermentation process, only a solvent'water 'is introduced, and almost no refining and impurity removing procedure is performed subsequently, so that risk substances such as ethanol and trichloromethane are not introduced while the economical efficiency is ensured, and the method is environment-friendly and safe.

This invention discloses a novel class of monoacylglycerol lipase (MAGL) small molecule inhibitors, as well as their pharmaceutically acceptable compositions, methods of preparation, and uses. The MAGL small molecule inhibitors are represented by formula (I), having the specific substituents and definitions described herein. The disclosed MAGL small molecule inhibitors exhibit excellent MAGL enzyme inhibitory activity. This invention includes these compounds or their pharmaceutically acceptable compositions for the treatment and / or prevention of MAGL-related conditions such as multiple sclerosis, Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis, traumatic brain injury, neurotoxicity, stroke, epilepsy, anxiety, migraine, depression, hepatocellular carcinoma, colorectal cancer lesions, ovarian cancer, neuropathic pain, chemotherapy-induced neuropathy, acute pain, chronic pain, and / or pain-related spasticity.

The invention discloses a pentapeptide VE5 with xanthine oxidase inhibitory activity and a preparation method and application thereof, and belongs to the technical field of small molecule peptides. The amino acid sequence of the pentapeptide VE5 is VSIVE, and the pentapeptide VE5 can be prepared through a solid-phase synthesis method and an enzymolysis method. The pentapeptide VE5 is identified from porphyra haitanensis proteolysis liquid and has potential interaction with xanthine oxidase, under the concentration of 0.1 mg / mL, the xanthine oxidase inhibition rate is 67.88%, and compared with goose carnosine (the xanthine oxidase inhibition rate is 36.03%), the xanthine oxidase inhibition rate is remarkably increased (plt; and the compound has higher xanthine oxidase inhibitory activity, and can be used for preparing a preparation for inhibiting xanthine oxidase activity and relieving hyperuricemia.

This invention discloses a mulberry leaf antihypertensive active peptide, its preparation method, and its application. Using mulberry leaves as raw material, this invention prepares mulberry leaf albumin. Enzymatic hydrolysis parameters, including hydrolysis time, pH, enzyme-to-substrate ratio, and substrate concentration, were optimized through single-factor and orthogonal experiments, providing optimal hydrolysis conditions for preparing crude ACE-inhibiting peptides. Further purification, peptide sequencing, and virtual screening identified highly active ACE-inhibiting peptides with strong solubility and good ACE-inhibiting activity. The two peptides with the highest activity, VPSCFDLTGK and RLPDFHGL, showed the highest IC50 values. 50 The values ​​were 8.23 ​​μmol / L (8.765 μg / mL) and 23.01 μmol / L (23.58 μg / mL), respectively. These bioactive peptides can act as angiotensin-converting enzyme inhibitory peptides, thereby lowering blood pressure by inhibiting ACE activity.

The invention relates to the technical field of bioinformatics and functional food development, and discloses a plant-source alpha-amylase inhibitory peptide high-throughput screening method and application thereof.The method comprises the steps that firstly, white kidney beans are selected and subjected to wall breaking and degreasing treatment, and efficient extraction is conducted; a three-stage gradient process is adopted for enzymolysis, and a series ultrafiltration membrane system is adopted for refining white kidney bean protein; separating white kidney bean protein, performing high-precision mass spectrum identification, screening peptide fragments, and constructing a candidate database; constructing a peptide-amylase molecular interaction screening network; collecting alpha-amylase inhibitory peptide data to carry out data enhancement, training a PAMIS-Net model, and carrying out model performance optimization; inputting the optimized PAMIS-Net model into the database in batches to intelligently screen high-activity candidate peptide fragments, and establishing a comprehensive scoring model for experimental verification; according to the method, the problems of low screening efficiency and poor prediction precision of the active peptide caused by difficulty in integration of multi-dimensional information such as sequences, structures and physicochemical properties in the prior art are solved.

The application belongs to the field of antitumor drug chemistry, and discloses application of a selective PRMT4 inhibitor, deacetylganoderic acid F, in a drug for resisting drug-resistant osteosarcoma. The deacetylganoderic acid F has the following structure: it forms a unique hydrogen bond effect and binding mode with PRMT4, is a PRMT4 selective inhibitor, has the characteristics of strong enzyme inhibition selectivity, small toxic and side effects, and strong anti-drug-resistant osteosarcoma effect, and can be used as an anti-drug-resistant osteosarcoma drug. Mechanism research shows that the deacetylganoderic acid F can regulate the active oxygen level to play an anti-drug-resistant osteosarcoma role. The problems of poor selectivity and large toxic and side effects of existing PRMT4 inhibitors are solved, and a new drug selection is provided for the treatment of drug-resistant osteosarcoma.

This invention belongs to the field of biomedical technology and discloses a specific structural lipase inhibitor that promotes ATGL activation, its preparation method, and its application. The inhibitor is derived from grape leaves. Through optimized extraction processes, the lipase inhibitory activity is significantly improved. The compound composition and structural ratio of the inhibitor are directionally enriched and clarified, resulting in a product with stable activity and controllable quality. Experiments have confirmed that the lipase inhibitor described in this application can simultaneously inhibit fat absorption and activate ATGL, forming a dual mechanism of action of "inhibiting absorption" and "inhibiting storage." It reduces TG, TC, LDL-C, LP, and FFA, upregulates HDL-C, stabilizes leptin, reduces ghrelin, and increases CCK and PYY, thereby effectively regulating lipid metabolism, controlling weight, improving blood lipids, and stabilizing blood sugar, with high safety.

This invention belongs to the field of biomedical technology, specifically relating to phosphodiesterase 2 (PDE2) activity inhibitors. Six PDE2 activity inhibitors were screened, providing six compounds: sanguisorbin, Picropodophyllol, aristolochic acid D, Malabaricone A, tetradehydropodophyllotoxin, and Roseoflavin. These compounds can be used to prepare PDE2 activity inhibitor drugs. Biological experimental methods were used to detect and verify the activity, resulting in effective PDE2 enzyme inhibitors. The IC50 level of these inhibitors was measured. 50 It exhibits good PDE2 enzyme inhibition effect.

The present invention relates to a bicyclic-type MAT2A inhibitor and use thereof. Specifically, the present invention discloses a bicyclic compound represented by formula (I) or a pharmaceutically acceptable salt, an enantiomer, a diastereomer, a racemate, an atropisomer, a polymorph, a solvate, or an isotope labeled compound thereof. The compound represented by formula (I) has MAT2A enzyme inhibitory activity, can be used as a good MAT2A inhibitor, and is further used for preparing drugs for treating and / or preventing MTAP-related diseases, especially tumors.

The application discloses application of a diphenyl ether compound in preparation of a beta-glucuronidase inhibitor. The diphenyl ether compound is obtained from a fungus Aspergillus versicolor ZJUTE2 through a series of processes such as organic solvent extraction and chromatographic column separation, simple extraction and separation, and has the advantages of simple preparation method, rapidness, high purity of obtained compound and the like; the diphenyl ether compound extracted by the application has good beta-glucuronidase inhibitory activity, and an IC 50 value of 56.59+ / -1.79 muM, is equivalent to a positive drug D-glucaric acid 1,4-lactone, and can be used for treating drug-induced diarrhea caused by irinotecan or non-steroidal anti-inflammatory drugs. In addition, development of structure optimization based on the compound as a lead is of great significance for research and development of a novel drug for treating drug-induced diarrhea.

The present application relates to the technical field of polypeptide complex, and discloses an almond peptide-polyphenol complex and application thereof, wherein the almond peptide-polyphenol complex is obtained by compounding almond peptide and polyphenol, the amino acid sequence of the almond peptide from N-terminal to C-terminal is FPWLQ, and the molecular weight is 689.80 Da; the polyphenol is chlorogenic acid.The present application determines the inhibitory activity of the almond peptide-polyphenol complex on angiotensin converting enzyme, and the results show that the enzyme inhibitory activity of the complex is greatly improved compared with single almond peptide and polyphenol substance, which proves that the complex has good enzyme inhibitory activity and can be effectively applied to the development of antihypertensive drugs, realizes high value-added utilization of almond resources, and has important significance for promoting the sustainable development of the almond industry.