140 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.

An α-amylase inhibitory peptide. The peptide comprises amino acid sequences of eight adjacent amino acids X1, X2, X3, X4, X5, X6, X7, and X8, wherein each amino acid of the peptide is independently selected from a D-amino acid or an L-amino acid, and at least one of X2, X4, and X6 is W. The peptide has α-amylase inhibitory activity, has the effects of losing weight and lowering blood sugar, and can be used for preparing α-amylase inhibitors, weight-losing drugs, hypoglycemic drugs, or foods, health-care products or drugs for preventing or treating obesity-related diseases.

The invention discloses camel milk polypeptide with xanthine oxidase inhibitory activity and application thereof.The camel milk polypeptide is prepared by taking fresh camel milk as a raw material, conducting low-temperature centrifugation to remove fat, conducting triple enzymolysis through papain, pepsin and trypsin to obtain enzymatic hydrolysate, enabling the enzymatic hydrolysate to pass through an ultrafiltration membrane (the molecular weight cutoff is 10 kDa) to obtain filtrate, and conducting freeze-drying to obtain the camel milk polypeptide. The compound has xanthine oxidase inhibitory activity. The invention also discloses a small molecule polypeptide with xanthine oxidase inhibitory activity. The filtered solution is screened and combined with polypeptides by adopting a xanthine oxidase affinity ultrafiltration method, the activity of the polypeptides is verified through molecular docking and in-vitro enzyme inhibition, four small-molecule polypeptides with xanthine oxidase inhibitory activity are obtained, the sequence of the small-molecule polypeptides is shown as any one of SEQ ID NO.1-4, and the small-molecule polypeptides can be used for preparing drugs with the effect of inhibiting the uric acid level.

The invention relates to the technical field of biology, in particular to a DPP-IV inhibitory peptide extracted from buffalo cheese protein hydrolysate and application of the DPP-IV inhibitory peptide. An active component with the molecular weight smaller than 3 kDa is obtained through alkaline protease enzymolysis, ultrafiltration separation and LC-MS / MS identification, and the DPP-IV enzyme inhibitory activity IC50 value of the active component is 12.6 mg / mL. Four new DPP-IV inhibitory peptide fragments are found, are amino acid sequences in a sequence table SEQ ID NO: 1-4, have good DPP-IV inhibitory activity, and have good application prospects in being developed into functional foods or medicines for regulating blood sugar. In conclusion, the enzymolysis product and the peptide fragment can be prepared into antidiabetic drugs or functional foods, and have the advantages of being natural, safe and efficient. The invention provides a new strategy for high-valued utilization of buffalo milk resources and treatment of type 2 diabetes.

The invention discloses a method for preparing various bioactive peptides based on bean dreg fermentation, which comprises polypeptides with alpha-glucosidase inhibitory activity, angiotensin converting enzyme inhibitory activity and antioxidant activity, and belongs to the field of microbial biological fermentation. Bacillus amyloliquefaciens sourced from fermented soybeans is used for fermentation, and a mixed product with alpha-glucosidase inhibitory activity, angiotensin converting enzyme inhibitory activity and antioxidant activity is obtained. The invention also provides a method for purifying the polypeptide with alpha-glucosidase inhibitory activity, angiotensin converting enzyme inhibitory activity and antioxidant activity, which is characterized in that the mixed product is purified by combined column chromatography, the combined column chromatography comprises cation exchange resin LXP-01, macroporous adsorption resin HP20, weak base anion exchange resin D941, silica gel resin and Sephadex LH-20. The invention also discloses seven bioactive peptides with biological activity, the amino acid sequences are CKLLL, APGYSC, FPKYG, FPGPLV, FPRSH, FMAV and SVCC, and the bioactive peptides have good alpha-glucosidase inhibitory activity, angiotensin converting enzyme inhibitory activity and antioxidant activity, and can be used for producing functional foods, health care products, cosmetics and the like for assisting in reducing blood sugar, reducing blood pressure, resisting oxidation and the like.

The present invention discloses a naphthalimide guanidine derivative, a preparation method thereof and an application thereof. The structural formula of the naphthalimide acyl guanidine compound is shown as formula (I), denoted as CAUZL-C; in formula (I), R is halogen, hydrogen, piperidyl or dimethylamino; n is 1, 2, 3 or 4. The naphthalimide guanidine derivative or a pharmaceutically acceptable salt thereof according to the present invention has good target enzyme inhibitory activity and insecticidal activity.

According to the preparation method disclosed by the invention, the whole fruit juice of the lonicera caerulea (which retains fruit residues) is fermented by virtue of the plant lactobacillus KLDS1.0391, KLDS1.0320 or KLDS1.0368, so that the xanthine oxidase (XO) inhibition activity is remarkably improved. After fermentation, the XO inhibition rate is increased to 48-50.87% (the content of unfermented juice is 31.21%), the total phenol content is increased by 15-24.3%, and the contents of main XO inhibitors in the lonicera caerulea: cyanidin-3-O-glucoside (IC50 = 115.28 [mu] M), cyanidin-3, 5-diglucoside (IC50 = 116.34 [mu] M), peonidin-3-glucoside (IC50 = 105.34 [mu] M), quercetin (IC50 = 88.75 [mu] M), catechin (IC50 = 110 [mu] M) and caffeoylquinic acid (IC50 = 250.35 [mu] M) are remarkably increased. Wherein the quercetin content is increased by 73.8% at most (KLDS1.0320 strain fermentation is performed for 24 hours), and the XO inhibition rate is increased from 31.21% to 50.87%. Technical support is provided for development of a natural XO inhibitor and a functional fermented beverage, so that a new thought is provided for functional fermented juice with lonicera caerulea as a key component.

The invention belongs to the technical field of biological medicine, and particularly relates to a novel deuterated JAK2 inhibitor or pharmaceutically acceptable salt thereof. Compared with the prior art, the compound or the pharmaceutically acceptable salt thereof provided by the invention has better JAK2 inhibition activity, and the JAK2 inhibition target selectivity of the compound or the pharmaceutically acceptable salt thereof is obviously superior to that of the existing compound, so that the compound or the pharmaceutically acceptable salt thereof has better druggability.

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 present invention relates to inhibitor compounds and aims to provide an acetohydroxyacid synthase inhibitor, a preparation method therefor, and a use thereof as an herbicide. The structure of the compound is shown in formula (I), and said compound specifically inhibits the activity of acetohydroxyacid synthase or a mutant thereof W574L in plants. The present invention further provides a method for applying said compound as an agrochemical herbicide. The described compound exhibits good enzyme inhibitory activity against wild-type acetohydroxyacid synthase and / or a mutant thereof W574L, and therefore can be used as an agrochemical herbicide for the control of various weeds in the agricultural field. Moreover, the compound can be used as both a pre-emergence and post-emergence herbicide, targeting various field weeds, and is particularly effective in controlling the malignant weed Leptochloa chinensis. The described compound features low dosage, excellent herbicidal activity, broad weed control spectrum, good translocation, wide application window, and safety to rice.

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.

The present invention belongs to the technical field of medicines. The present invention relates to an imidazolidinedione HDAC inhibitor, and a preparation method therefor and the use thereof. Provided in the present invention is an imidazolidinedione HDAC inhibitor, which inhibitor is a substituted imidazolidinedione compound as represented by general formula V, or a stereoisomer, a hydrate or a pharmaceutically acceptable salt thereof. The inhibitor has efficient and good HDAC enzyme inhibitory activity, and also has good in-vitro anti-tumor activity. The inhibitor provides a new way for the application of an HDAC inhibitor in tumors / or the treatment of diseases related to uncontrolled histone deacetylase activity.

The present invention discloses a method for preparing milk-derived angiotensin-converting enzyme inhibitory peptides by fermentation with composite strains, which belongs to the fields of microbial technology and fermentation. The ratio of whey protein hydrolysate with a molecular weight below 1000 Da and the angiotensin-converting enzyme inhibition rate in the milk-based fermentation broth are used as evaluation indicators. The composite strain Lactobacillus helveticus ( Lactobacillus helveticus , CICC: 20289), composite strain Pediococcus dilactici ( Pediococcus acidilactici , CICC:20719) were rescreened to obtain strains with excellent whey protein hydrolysis performance and high angiotensin-converting enzyme inhibitory peptide production capacity. The two composite strains obtained from the rescreening were enriched and cultured separately, and then inoculated into skim milk powder culture medium at a specific compound ratio. Through composite fermentation, the angiotensin-converting enzyme inhibitory peptide content in the milk-based fermentation product was increased. The process of this invention is rationally designed and highly operable. It provides a reference for further increasing the content of small molecule functional peptides in fermented dairy products, efficiently preparing milk-derived angiotensin-converting enzyme inhibitory peptides, and improving the nutritional value of dairy products, and has great application prospects.

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;

This invention relates to the technical field of deep processing of rye pollen, and particularly to a rye pollen peptide with antioxidant, anti-glycation, and α-amylase inhibitory activities, its preparation method, and functional products. The preparation method includes the following steps: mixing rye pollen with water, then sequentially adding cellulase and pectinase for pretreatment; after enzyme inactivation in the pretreatment solution, sequentially adding Bacillus licheniformis alkaline protease, papain, and Bacillus subtilis neutral protease for three hydrolysis cycles; and obtaining powdered rye pollen peptides after solid-liquid separation, filtration, and drying. The rye pollen peptides prepared by the method of this invention possess antioxidant, α-amylase inhibitory, and anti-glycation activities, and also have prebiotic effects that promote the proliferation of *Lactobacillus plantarum* and *Lactobacillus fermentum*.

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 relates to a novel N-(2-(4-cyano thiazolidine-3-yl)-2-oxyethyl) quinoline-4-formamide derivative and a preparation method of the N-(2-(4-cyano thiazolidine-3-yl)-2-oxyethyl) quinoline-4-formamide derivative. The structure of the compound or the pharmaceutically acceptable salt is C-A-B, A is a quinoline ring, B is an (R)-3-glycyl thiazolidine-4-nitrile side chain, and C is a side chain containing a sulfoximine structure. The compound or the pharmaceutically acceptable salt of the compound, and the pharmaceutical composition containing the compound or the pharmaceutically acceptable salt of the compound have obvious FAP enzyme inhibition activity, and can be used for preparing an FAP small-molecule inhibitor.

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.