521 results about "Enzyme inhibitor" patented technology

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.

Provided herein are certain fused ring compounds, such as a compound of Formula (A), as Werner Syndrome RecQ DNA helicase (WRN) inhibitors, pharmaceutical compositions comprising the compounds, and method of use of the compounds or pharmaceutical compositions in the treatment of diseases or disorders.

The invention discloses a tyrosinase inhibitory peptide from kelp as well as a preparation method and application of the tyrosinase inhibitory peptide. The preparation method comprises the following steps: pretreating kelp, fermenting the kelp by using lactobacillus plantarum, carrying out centrifugation, ultrafiltration and component identification on the obtained fermentation liquor to obtain the composition of kelp polypeptide, screening the tyrosinase inhibitory peptide through molecular docking, and finally carrying out solid-phase synthesis to obtain the tyrosinase inhibitory peptide prepared by the invention. The lactobacillus plantarum fermentation technology is simple and feasible, the production cost is low, equipment is easy to obtain, active ingredients in kelp can be released to the maximum extent, and the prepared polypeptide has the effect of inhibiting the activity of tyrosinase and can be used for developing a tyrosinase inhibitor.

The invention discloses application of a lysosome cathepsin L inhibitor in a medicine for treating or relieving allergic airway inflammation, and relates to the field of allergic airway inflammation. It is found through research that inflammatory response of asthma can be relieved by inhibiting expression of lysosome CTSL in macrophages and animal models; the inflammatory response of asthma can be relieved by inhibiting expression of lysosome CTSL in macrophages by using a small-molecule inhibitor and myeloid specific knockout CTSL, so that the lysosome cathepsin L inhibitor can effectively relieve allergic airway inflammation, and a new direction can be provided for research and development of drugs for treating and relieving allergic airway inflammation in the future.

The invention discloses a preparation method of deer spleen aminopeptide powder in the field of bioactive substance extraction and functional material compositing, and the performance of the deer spleen aminopeptide powder is improved by compositing a multi-stage functional modified material and deer spleen aminopeptide. The preparation method comprises the following steps: cleaning, homogenizing and crushing fresh deer spleen, extracting with a phosphate buffer solution, adjusting the pH value, carrying out enzymolysis, inactivating enzyme, and treating with an ultrafiltration membrane and a nanofiltration membrane in a specific molecular weight range to obtain a concentrated solution; and mixing the concentrated solution with a multi-stage functional modified material under proper conditions, sterilizing, pre-freezing, and freeze-drying to obtain the deer spleen aminopeptide powder. Wherein the modified material is constructed through quaternization modification, nanopore loading, enzyme inhibitor coupling and targeting ligand modification, and has the functions of charge repulsion, steric hindrance, enzyme inhibition and targeting recognition. The deer spleen aminopeptide powder prepared by the invention has high stability and good bioavailability, and is suitable for functional food or health care products.

The invention relates to the technical field of plant tissue extraction, in particular to an efficient extraction method and application of ginseng callus-derived exosomes, the extraction method comprises the following steps: S1, mixing ginseng callus with a PBS buffer solution, homogenizing and filtering to obtain a filtrate; s2, adding a protease inhibitor and a deep eutectic solvent into the filtrate, uniformly mixing, and standing to obtain a mixed solution; s3, centrifuging and filtering the mixed solution, and reserving supernate; s4, carrying out ultracentrifugation on the supernatant, collecting the precipitate, and resuspending with PBS to obtain a resuspension; and S5, further filtering the resuspension to obtain a filtrate, and storing at low temperature. The ginseng callus exosome extracted by the extraction method disclosed by the invention can be applied to preparation of drugs or cosmetics with anti-oxidation, anti-inflammatory and anti-aging effects, and the technical problems of low extraction efficiency, insufficient purity, complex extraction operation and poor stability of the extracted exosome in the existing exosome extraction technology can be effectively solved.

The invention discloses preparation of immobilized alpha-glucosidase based on a magnetic metal organic framework (MOF) and application of the immobilized alpha-glucosidase in screening of natural enzyme inhibitors. According to the method, ZIF-90 is grafted on the surfaces of Fe3O4 magnetic nanoparticles modified by codeposition of polydopamine and polyethyleneimine, and alpha-glucosidase is synchronously encapsulated in situ in the growth process of the ZIF-90, so that the magnetic MOF immobilized alpha-glucosidase is successfully constructed. On the application level, an in-vitro enzyme inhibition activity evaluation system is constructed, multiple traditional Chinese medicine extracts are selected as research objects, and by means of the characteristic that the magnetic MOF immobilized alpha-glucosidase is easily separated from a reaction system, accurate screening of natural inhibitors or active small molecules is rapidly and efficiently achieved; and a novel screening method is provided for research and development of candidate drugs for diabetes mellitus. The method comprises the following steps: 1, preparing the magnetic MOF immobilized alpha-glucosidase and evaluating the performance of the magnetic MOF immobilized alpha-glucosidase; and 2, the prepared immobilized alpha-glucosidase is used for screening a natural enzyme inhibitor. Based on a magnetic MOF immobilized enzyme technology, the method provided by the invention has the characteristics of rapidness, high efficiency, accuracy, easiness in separation from a reaction system and reutilization of a target receptor alpha-glucosidase, is suitable for screening of alpha-glucosidase inhibitors in complex systems such as traditional Chinese medicines, and has a wide application prospect.

Provided herein are certain aminoheteroaryl compounds with tricyclic structure moiety, pharmaceutical compositions, and methods of use related to cyclin dependent kinases (CDKs). The compounds provided herein are typically CDK4 inhibitors, which can be used for treating a variety of diseases or disorders, such as cancer.

The invention discloses a small molecule peptide with xanthine oxidase inhibitory activity and application thereof, and belongs to the technical field of bioactive peptides. The amino acid sequence of the small molecule peptide with xanthine oxidase inhibitory activity is YDWRPF, and is as shown in SEQ ID NO. 8. The small molecule peptide with the xanthine oxidase inhibitory activity is applied to preparation of a xanthine oxidase inhibitor. The small molecule peptide YDWRPF is high in xanthine oxidase inhibitory activity, IC50 is only 2.73 + / -0.20 mM, and the small molecule peptide YDWRPF can be used as a raw material to prepare a xanthine oxidase inhibitor. The invention is of great significance to the treatment of hyperuricemia.

The present invention belongs to the technical field of genetic engineering. Provided are a single-base editor, a deaminase used therein, and the use thereof. The technical problems to be solved are to identify a naturally occurring cytosine deaminase without sequence preference, construct a base editor, and improve the efficiency and scope of base editing. In order to solve the technical problems above, a cytosine base editor is provided. The cytosine base editor is a fusion protein, wherein the fusion protein is a protein containing a cytidine deaminase, a Cas protein and a uracil-DNA glycosylase inhibitor, and the cytidine deaminase is a protein having an amino acid sequence of positions 28-164 of SEQ ID NO. 2. Further provided is the use of the fusion protein above and a biomaterial related thereto in plant single-base editing. The single-base editor can improve the efficiency of cytosine base editing and accurately mediate the base mutation of a target, and is widely applicable in the cells of maize and even other plants.

The invention belongs to the technical field of food additives and new materials, and discloses a thermostable embedding method and application of an alpha-amylase inhibitor, and the method comprises the following steps: respectively adjusting the pH values of an alpha-AL stock solution and an iota-CG stock solution to 6, then mixing the stock solutions according to the mass ratio of alpha-AL to iota-CG of 2: 1, and carrying out heat preservation for 2-3 hours, so as to obtain the thermostable embedding method of the alpha-amylase inhibitor. According to the method disclosed by the invention, the stable ion compound is formed under the condition that the pH is equal to 6 by utilizing the electrostatic interaction and the hydrogen-bond interaction between the negatively charged sulfuric acid group in the iota-carrageenan molecule and the positively charged amino acid residue on the surface of the white kidney bean alpha-amylase inhibitor. According to the compound, stable combination among molecules is achieved by constructing a structured water molecular layer barrier, so that the tolerance of the white kidney bean alpha-amylase inhibitor to heat treatment is remarkably improved, and the defect that the heat stability of the white kidney bean alpha-amylase inhibitor is poor is overcome.

The invention belongs to the field of medical chemistry, and particularly discloses a protein tyrosine phosphatase inhibitor, such as type 2 non-receptor protein tyrosine phosphatase (PTPN2) and / or type 1 non-receptor protein tyrosine phosphatase (PTPN1) inhibitor, a pharmaceutical composition and application thereof. The invention discloses a method for treating related diseases such as cancers and metabolic diseases by using the protein tyrosine phosphatase inhibitor.

The invention provides a method for detecting an anti-C1 esterase inhibitor neutralizing antibody in a biological sample, and the method mainly utilizes the characteristic that protein A resin is combined with an Fc segment of the antibody to capture the antibody (containing the anti-C1 esterase inhibitor neutralizing antibody), so that the C1 esterase inhibitor and complement component 1s (C1s) in the biological sample after thermal inactivation are removed; furthermore, an antibody (containing a neutralizing antibody) or an anti-C1 esterase inhibitor compound on the protein A resin is subjected to acid dissociation through an acidolysis solution, so that not only can the anti-C1 esterase inhibitor neutralizing antibody existing in a free form in a biological sample be detected, but also the anti-C1 esterase inhibitor neutralizing antibody existing in a combined form in the biological sample can be detected.

The invention discloses an anti-leaching nutrient slow-release synergistic compound fertilizer, and particularly discloses an anti-leaching nutrient slow-release synergistic compound fertilizer and a preparation method thereof. The compound fertilizer comprises the following components in parts by weight: 30-50 parts of urea particles, 15-25 parts of monoammonium phosphate, 20-30 parts of potassium sulfate, 2-5 parts of a slow-release synergistic coating agent, 1-3 parts of a bonding wrapping layer and 10-20 parts of a filling material. The slow-release synergistic coating agent comprises polyaspartic acid (PASP) and a composite inhibitor (a urease inhibitor and a nitrification inhibitor), and the bonding wrapping layer is made of a polyvinyl alcohol / sodium polyethylene acid-based cementing material. The preparation method comprises the following steps: mixing and granulating raw materials, carrying out primary coating (slow-release synergist), carrying out secondary coating (bonding a coating layer), and drying and screening. Through the synergistic effect of the double coating technology and the compound inhibitor, the nitrogen conversion and release are obviously delayed, the nutrient leaching loss is reduced by 20-40%, the fertilizer utilization rate is improved by 25-30%, and the compound fertilizer is suitable for high-temperature and rainy areas.

The invention provides a compound serving as a glutamine cyclase inhibitor and application of the compound, and belongs to the field of medical chemistry. The structure of the compound is shown as a formula I. The compounds have good inhibitory activity on sQC and gQC enzymes and mutants thereof, and the half inhibitory concentration of most compounds reaches the sodium mole level, so that the compounds can be used for preparing glutamine cyclase inhibitors. In addition, the compounds can also be used for preparing medicines for preventing and treating diseases related to glutamine cyclase. The invention lays a material basis for research and development of glutamine cyclase inhibitor drugs, and has a good application prospect. Formula I.

The invention relates to the field of food processing, and particularly discloses composite yeast for low-GI bread, a preparation method of the composite yeast and the low-GI bread. The low-GI bread composite yeast comprises the following raw materials in parts by weight: 4-5 parts of saccharomyces cerevisiae, 3-5 parts of lactobacillus plantarum, 1-2.5 parts of pediococcus pentosaceus, 100-150 parts of solid state fermentation pomace powder, 0.1-0.5 part of an enzyme inhibitor and 25-40 parts of millet resistant starch. The compound yeast is used for preparing the bread with the low GI value, and the prepared bread is low in glycemic index, good in expansibility, large in size, good in water binding capacity and not prone to hardening.

Compounds and methods are provided for inhibiting a PI4-kinase. Methods of treating a pathogen infection and methods of treating cancer are also provided. The PI4-kinase inhibitor can be a compound that is a 5-aryl or heteroaryl-thiazole, e.g., as described herein. In certain embodiments, the PI4-kinase inhibitor is a substituted 2-amino-5-phenylthiazole or substituted 2-amino-5-pyridylthiazole compound. In some embodiments, the compounds have broad spectrum anti-infective activity against a variety of infective diseases, where the diseases are caused by pathogens containing a basic amino acid PIP-2 pincer (BAAPP) domain that interacts with phosphatidylinositol 4,5-bisphosphate (PIP-2) to mediate pathogen replication. Also provided are methods of treating a subject for cancer using a PI4-kinase inhibitor. Aspects of the methods include inhibiting PI4-kinase in a cancer cell to reduce cellular proliferation.

The present invention provides a method for detecting the presence of or risk of bladder cancer in a female patient, the method comprising the steps of: detecting the presence of a biomarker panel in a sample isolated from a female patient, the biomarker panel comprising IL-13 and IL-12p70 and one or more biomarkers selected from the group consisting of BTA, midkine, PAI-1 / tPA, 8OHdG, CEA, CK18, Fibrillin, Creatinine, CXCL16, Cystatin B, Cystatin C, d-dimer, EGF, FAS, HAD, IL-1a, IL-1b, IL-4, IL-6, IL-7, IL-8, MCP-1, Microalbumin, MMP9 NGAL, MMP9 TIMP1, NGAL, NSE, Progranulin, TUP, TGFB1, Thrombomodulin, sTNFR1, TPA, VEGF and Triglyceride, and / or the concentration of albumin / microalbumin / protein to creatinine in a sample isolated from a female patient, expressed as an albumin:creatinine ratio; and assessing the result and comparing it to a normal control, wherein an increase in the presence of the biomarkers compared to the normal control indicates the presence or risk of cancer in the patient from which the sample was isolated.

This invention relates to a 1,3,4-thiadiazole peptide deformylase inhibitor and its preparation and application. The structural formula is shown in formula (1): wherein, R 1 It is n-butyl or cyclopentylmethyl; R 2 The compounds are hydrogen-containing, straight-chain alkanes, cyclic alkanes, aromatic rings, substituted biphenyls, or heterocyclic rings. The 1,3,4-thiadiazole peptide deformylase inhibitors provided by this invention can effectively inhibit bacterial protein synthesis, thereby achieving sterilization. These compounds exhibit excellent inhibitory activity against Gram-positive drug-resistant bacteria, especially the clinically challenging methicillin-resistant Staphylococcus aureus (MRSA). In particular, some preferred compounds show inhibitory activity 4-8 times that of the control standards vancomycin and linezolid. The 1,3,4-thiadiazole peptide deformylase inhibitors provided by this invention also exhibit inhibitory activity against Gram-negative drug-resistant bacteria, especially against drug-resistant Acinetobacter baumannii, known as "superbugs," with an inhibitory activity reaching 0.5 μg / mL, far superior to vancomycin and linezolid.

The present invention discloses the application of Ganoderma lucidum lanostane triterpenoids in the preparation of CYP metabolic enzyme inhibitors, belonging to the technical field of pharmaceuticals. The structural formula of this compound is as follows: #imgabs0# The present invention also provides the application of lanostane triterpenoids in the preparation of CYP metabolic enzyme inhibitors, and evaluates their inhibitory effects on various subtypes of CYP enzymes and the intervention of drug metabolism. The lanostane triterpenoids provided by the present invention can effectively inhibit the activities of various CYP metabolic enzymes, and can be used as combination drugs in inhibiting the hepatic metabolism of clinical drugs, providing a reference for the clinical use of Ganoderma lucidum.

The present invention comprises one or more organic solvents that create a non-aqueous organo solvent delivery system, (NOSDS), and one or more Organo Polycarboxylate functionalities, OPCF, that results in a stable, non-aqueous solution that can easily, safely, evenly and economically coat nitrogen source granules and / or be added to a mobile liquid form of a nitrogen source such as an aqueous dispersion, pressurized ammonia gas or molten urea and / or molten modified urea. Using these solvents provides more flexibility for nitrogen source manufacturers to produce nitrogen sources designed for a particular soil or plant. The liquid solutions are comprised of NOSDS and OPCFs and one or more of a) nitrification inhibitors, b) urease inhibitors, c) pesticides, d) fungicides, e) herbicides, f) insecticides and g) micronutrients.

The invention relates to a method for producing particles comprising urea and at least one urease inhibitor and / or at least one nitrification inhibitor, and to a suitable apparatus for carrying out the method.

The invention discloses an immunostaining reagent for MHC-II expression detection of a gastric cancer biopsy sample, and belongs to the field of bioengineering. The invention establishes a preparation method of an immunohistochemical staining section. The preparation method specifically comprises the following steps: step 1, early-stage treatment: baking a tissue section, dewaxing, rehydrating, subsequently adding an antigen solution for repairing, adding an endogenous enzyme inhibitor for incubation, adding a sealing agent for sealing and the like; step 2, antibody incubation: adding a first antibody and a second antibody for incubation; and step 3, post-treatment: dyeing, re-dyeing, bluing, sealing and the like. A mixed buffer solution is used as an endogenous enzyme inhibitor, so that the background staining intensity is effectively reduced, and the staining sensitivity and specificity are improved; meanwhile, a staining result interpretation standard is established, it is proved that MHC-II expression is remarkably related to pathological remission of the gastric cancer patient, and an evaluation method is provided for pathological remission of the gastric cancer patient.

The present application relates to "application of a compound in soybean cyst nematode chitinase inhibitor", belong to the technical field of leguminous plant symbiotic protection, the application of the compound and its pharmaceutically acceptable salt in soybean cyst nematode chitinase inhibitor, the present application is evaluated and researched through the inhibitory activity of compound by screening work, the inhibitor is screened finally, the inhibitor is likely to have good application prospect in controlling soybean cyst nematode disease aspect.The present application also provides a kind of chitinase inhibitor with the function of inhibiting the establishment of symbiosis of soybean cyst nematode to destroy, the number of nodule obtained by processing is flat with the number when only inoculating rhizobium, the inhibitory effect of Hg-CHI-1 on rhizobium nodule is completely restored, and it has good application prospect in the aspect of leguminous plant symbiotic protection.

This invention discloses the XO-inhibiting peptide GDEY and its applications, belonging to the field of bioactive peptide technology. The amino acid sequence of the XO-inhibiting peptide GDEY is shown in SEQ ID NO.2. The invention also discloses the application of the XO-inhibiting peptide GDEY in the preparation of xanthine oxidase inhibitors and in the preparation of drugs with the effect of inhibiting uric acid levels. This invention used molecular docking and BLAST+ software to virtually screen 15 potential XO-inhibiting peptides from the complete protein sequence of Litopenaeus vannamei. High-performance liquid chromatography (HPLC) was used to determine the XO-inhibiting activity, and the results showed that 7 small molecule peptides exhibited significant XO-inhibiting activity, possessing potential value in preventing hyperuricemia.

The invention belongs to the technical field of animal skin processing, and discloses an oxidation-assisted sheepskin enzyme unhairing method, which comprises the following steps: in a sheepskin unhairing process, firstly adding protease to carry out enzyme unhairing, after the protease fully permeates into the skin, adding a protease inhibitor to inhibit the protease activity on the surface of the skin, and when the unhairing area reaches 80-90%, stopping unhairing; and carrying out oxidation depilation under an alkaline condition by using a strong oxidant until the depilation is completed. According to the method, the acting time and acting strength of protease on sheepskin surface collagenous fibers are reduced, meanwhile, wool at the positions such as the back and the side belly of the sheepskin is completely removed, the problems that when an existing enzyme unhairing technology is used for the sheepskin, unhairing is incomplete, and the sheepskin collagenous fibers are seriously damaged are solved, and high-quality unhaired bare skin can be obtained. The sheepskin unhairing method is convenient to operate, mild in condition and environmentally friendly, and the prepared unhaired bare skin can be used for industries such as leather making and food.

Disclosed herein is a method of modifying a T cell during T cell activation comprising contacting the T cell with an inhibitor of prolyl hydroxylase. Also disclosed is a method of producing a chimeric antigen receptor (CAR) or T cell receptor (TCR) T cell comprising (i) modifying the T cell during activation of the T cell by contacting the T cell with an inhibitor of prolyl hydroxylase, (i) introducing a CAR or TCR transgene into the modified T cell, and (iii) harvesting the CAR or TCR T cell. In particular, the inhibitor of prolyl hydroxylase is a small molecule prolyl hydroxylase inhibitor, such as 1, 4-DPCA. The harvested CAR or TCR T cells can be used for adoptive T cell immunotherapy of cancer.

The invention discloses a semeglutide capsule and a preparation method thereof.The semeglutide capsule comprises a pill core, a coating layer and a capsule shell, the pill core is coated with the coating layer, the capsule shell is filled with the pill core coated with the coating layer, and the total mass percentage of the pill core and the coating layer is 100%. The pellet core is prepared from the following components in percentage by weight: 0.43 to 0.85 percent of semeglutide, 19.94 to 37.04 percent of an absorption enhancer, 4.84 to 8.26 percent of an enzyme inhibitor, 14.25 to 22.79 percent of an adhesive, 19.66 to 44.01 percent of a shaping agent and 2.85 to 4.56 percent of an adhesive; and the coating layer comprises the following components in percentage by weight: 7.41 to 10.83 percent of a film forming agent, 0.28 to 0.57 percent of a plasticizer and 0.56 to 1.14 percent of an emulsifying agent. The capsule disclosed by the invention can target colon, and does not need fasting before and after taking medicine, so that the bioavailability of the semeglutide is greatly improved, and the production cost of the preparation is reduced.

The present invention relates to a novel crystalline form of a helicase-primase inhibitor compound, and to pharmaceutical compositions comprising the novel crystalline form, to methods of production of the novel crystalline form, to the crystalline form in medicine and for use in the treatment of herpes viral infections.

The invention discloses a tea yellow liquid as well as a preparation method and application thereof, and belongs to the field of agricultural additives. The preparation process of the tea yellow liquid comprises the following steps: drying and crushing raw materials, adding water for dissolving out, centrifuging to obtain a mixed fine suspension, finally adding an enzyme inhibitor, and carrying out secondary sanding and dilution to obtain the tea yellow liquid. The tea yellow liquid is prepared from, by mass, 7-99.5% of tea saponin liquid, 0.5-93% of coptis chinensis liquid and the balance water, tea saponin active ingredients contained in the tea saponin liquid can remarkably reduce the surface tension of pesticide liquid, the tea saponin active ingredients cooperate with macromolecular substances such as polysaccharide in the coptis chinensis liquid to form a biomass affinity film, the spreadability and adsorbability of the pesticide liquid are greatly improved, and the pesticide effect is improved. Therefore, the content of the pesticide liquid in unit area is increased, the application amount of the pesticide is greatly reduced, and pesticide residues caused by excessive application are reduced.