658 results about "Inhibitory effect" patented technology

The invention relates to the technical field of microorganisms, in particular to nocardia seriolae bacteriophage as well as a composition and application thereof. The name of the nocardia seriolae bacteriophage is RDP-NS002, the nocardia seriolae bacteriophage is preserved in the China General Microbiological Culture Collection Center on August 25, 2025, and the preservation number of the nocardia seriolae bacteriophage is CGMCC No.46674. The nocardia seriolae bacteriophage is named as RDP-NS002, and the nocardia seriolae bacteriophage is preserved in the China General Microbiological Culture Collection Center on August 25, 2025. The composition comprises the bacteriophage. The bacteriophage or the composition is prepared in the following steps: (1) preparing a product for killing nocardia seriolae; (2) preparing a product for inhibiting nocardia seriola; and (3) application in preparation of a product for preventing and / or treating fish nocardia disease caused by nocardia seriolae. The phage has the characteristics of high thermal stability, high acid-base stability and high splitting rate, has a long-acting inhibition effect, and is beneficial to prevention and treatment of nocardia seriola diseases.

The invention provides a beta '-sulfo-alpha, beta-unsaturated gamma-lactam derivative as well as a preparation method and application thereof, and belongs to the technical field of organic chemical synthesis. The beta '-thio-alpha, beta-unsaturated gamma-lactam derivative has a structure as shown in a formula I. According to the method disclosed by the invention, cesium carbonate is taken as alkali, and a molecular skeleton of the beta'-thio-alpha, beta-unsaturated gamma-lactam derivative is constructed through free radical coupling and olefin isomerization processes under the condition of blue light irradiation. Bioactivity evaluation shows that the beta '-sulfo-alpha, beta-unsaturated gamma-lactam derivative prepared by the method disclosed by the invention has an inhibition effect on MDA-MB-231 human breast cancer cells.

The invention discloses an oligopeptide from undaria pinnatifida and application thereof. The amino acid sequence of the oligopeptide is YRKD, and the molecular weight is 580.63 g / mol. The polypeptide is identified from undaria pinnatifida through a high performance liquid chromatography technology for the first time, and an unreported oligopeptide capable of inhibiting tyrosinase and cooperating with vitamin C to synergistically inhibit tyrosinase is screened out. The oligopeptide derived from undaria pinnatifida is synthesized by a solid phase method, has the characteristics of safety, no toxicity, good water solubility and good stability, and is combined with vitamin C to generate a synergistic effect and synergistically increase the inhibition effect on tyrosinase, so that the oligopeptide can achieve a better tyrosinase inhibition effect at a lower and more stable concentration; the use concentration of the oligopeptide can be greatly reduced, the stability is enhanced, and the oligopeptide can be widely applied to preparation of cosmetics, medicines, health-care products or food additives, and has important economic value and social significance.

The invention discloses an application of imatinib mesylate in preparation of a targeted therapeutic drug for gastric signet ring cell carcinoma. The imatinib mesylate has an obvious inhibition effect on the growth of six patients with the pathological type of gastric signet-ring cell carcinoma, the inhibition effect is more obvious along with the increase of the concentration, the concentration and dosage dependency relationship is shown, and the half inhibitory concentration (IC50) is obviously smaller than that of a positive control drug apatinib. The medicine can play a targeted therapeutic role on the gastric signet ring cell carcinoma, and is small in toxic and side effects, economical, practical and low in cost.

The invention provides a method for analyzing interaction between procambarus clarkia arginine kinase and shark source nano antibody. The method comprises the following steps: performing three-dimensional structure prediction on a VNAR sequence, and screening a high-confidence VNAR model by using a Laplace map; docking an amino acid sequence corresponding to the VNAR model with an arginine kinase sequence to obtain an optimal compound model, and analyzing an interaction site of an arginine kinase epitope region and a nanometer antibody complementary determining region CDR3; performing molecular dynamics simulation on the compound model, calculating conformational change indexes and binding free energy through energy optimization, system balance and extended simulation sampling, and outputting a binding stability sequence of the nano antibody and arginine kinase; the method comprises the following steps: screening out a high-stability nano antibody, pre-incubating a fusion protein of the high-stability nano antibody and immobilized arginine kinase to form a compound, adding serum of an allergic patient for competitive binding, quantifying the binding activity of residual IgE through an immunodetection technology, and verifying the inhibition effect of the shark source nano antibody on the sensitization effect of arginine kinase.

Provided in the present invention are a compound as represented by formula (I), or a pharmaceutically acceptable salt, a tautomer, a geometrical isomer, an optical isomer, a solvate or an isotopic derivative thereof, and the use thereof. The compound of the present invention has a significant inhibitory activity on PRMT5, has a significant inhibitory effect on tumor cells and in vivo tumor models, also has a good administration performance, and has clinical application potential for preventing and / or treating diseases which are at least partially mediated by PRMT5.

The invention belongs to the technical field of prevention and treatment of rice blast, and particularly relates to a polypeptide MP1 for inhibiting rice blast bacteria and application thereof. The invention discloses a polypeptide MP1 for inhibiting magnaporthe oryzae. The amino acid sequence of the polypeptide MP1 is as shown in SEQ ID NO. 1. The polypeptide MP1 has an obvious inhibition effect on the magnaporthe oryzae appressorium, and the EC50 formed by the MP1 polypeptide on the appressorium is 134.60 mu M. Experiments show that the polypeptide can effectively interfere the normal differentiation and development of the appressorium in the key pathogenic stage of magnaporthe oryzae, so that the polypeptide has a strong prevention and control potential in the early stage of pathogenic bacterium infection. The polypeptide MP1 provided by the invention can significantly reduce the pathogenicity of magnaporthe oryzae to barley and rice, and provides an experimental basis for developing a novel biopesticide for preventing and treating the magnaporthe oryzae.

The invention relates to the technical field of polypeptide biosynthesis, in particular to a method for biosynthesizing acetyl tetrapeptide-5, a composition containing the acetyl tetrapeptide-5 and application of the composition. According to the method, low-cost natural amino acid is used as a substrate, specific aminopeptidase or a mutant thereof is used as a biocatalyst, amino acid ligase and polyphosphatase are combined, and acetyl tetrapeptide-5 can be efficiently synthesized through a one-step enzymatic reaction. Compared with a traditional chemical synthesis method, the method has the advantages of low raw material cost, no use of an organic solvent, mild reaction conditions, high regioselectivity, environmental friendliness, low production cost and the like. The invention also provides a composition containing acetyl tetrapeptide-5 and dipeptide-15, the inhibition effect of the composition on grease secretion is obviously better than that of a single component, and the composition has a synergistic oil control effect under a specific ratio.

The invention provides a preparation method and drug detection application of ZIF-8-Fe metal organic framework nano-enzyme, the ZIF-8-Fe metal organic framework nano-enzyme is prepared by adopting a heating reflux method, and peroxidase-like activity and drug detection application of the ZIF-8-Fe metal organic framework nano-enzyme are researched. In the presence of H2O2, the material can catalytically oxidize TMB to generate a blue product and shows good peroxidase activity, and through optimization experiments, proper reaction temperature and pH buffer system and optimal concentrations of ZIF-8-Fe, TMB and H2O2 are determined. Kinetic analysis shows that the affinity of TMB is superior to that of natural HRP, and a colorimetric detection method is established based on the inhibition effect of TC on the catalytic reaction. The method disclosed by the invention is reasonable in linear range, relatively low in detection limit and good in sample recovery rate and relative standard deviation performance, can be used for detecting tetracycline tablets, and shows a potential application value of the ZIF-8-Fe nano-enzyme in the field of drug detection.

The invention discloses tranexamic acid-polypeptide conjugate as well as a preparation method and application thereof, and belongs to the technical field of biology. The invention relates to a tranexamic acid-polypeptide conjugate or a salt thereof. The structure of the tranexamic acid-polypeptide conjugate is as shown in the following formula (I): TXA-Xaa1-L-phenylalanyl-D-arginyl-L-tryptophanyl-Xaa2-NH2 (I), wherein TXA-Xaa1-L-phenylalanyl-D-arginyl-L-tryptophanyl-Xaa2-NH2 (I) is shown in the description; wherein TXA is 4-(aminomethyl) cyclohexane carbonyl, and TXA is 4-(aminomethyl) cyclohexane carbonyl; xaa1 is a chemical bond, a neutral amino acid residue or a hydrophilic linker; xaa2 is a chemical bond, a neutral amino acid residue or a hydrophilic linker. The tranexamic acid-polypeptide conjugate or the salt thereof disclosed by the invention can simultaneously block two key signal channels for melanogenesis to achieve a synergistic effect of '1 + 1gt, 2', and further improve the inhibition effect on melanogenesis.

The present invention aims to provide a method for evaluating the serotonin reuptake inhibitory effect of a composition containing valerian extract. [Solution] The present invention provides a method for evaluating antidepressant effects, which involves quantitatively analyzing one or more components contained in at least a part of a plant of the genus Valerian or a processed product thereof, and evaluating the antidepressant effect of the test substance by referring to the results of the quantitative analysis and criteria for antidepressant effect.

This invention belongs to the field of organic synthesis and relates to a nitrogen-containing [3,2-b]indole derivative, its preparation method, and its application. The nitrogen-containing [3,2-b]indole derivative is a compound, optical isomer, or pharmaceutically acceptable salt thereof, as shown in the following structure: ; wherein R1, R2, R3, and R4 are independently selected from hydrogen atoms, halogens, cyano groups, C1-C8 alkyl groups, and C1-C8 alkoxy groups; R5, R6, R7, and R8 are independently selected from hydrogen atoms, halogens, and C1-C8 alkyl groups; R9 is selected from C1-C8 alkyl groups; when R1, R2, R3, R4, R5, R6, R7, and R8 are all hydrogen atoms, R9 is selected from C1-C2 alkyl groups. The compound exhibits antitumor activity, particularly against HeLa cervical cancer, showing a significant inhibitory effect on its proliferation.

This invention provides an application of the peptide Nod-T3 in the preparation of drugs for treating lung diseases. The Nod-T3 peptide is derived from human protein and has a significant inhibitory effect on chronic lung inflammation and fibrosis caused by smoking. It can be used to treat COPD and other smoking-related lung diseases. It also has high biocompatibility and low toxicity, and has the potential and development value to become a new type of peptide drug.

The present invention provides topical and internal skin preparations containing an extract of soapwort cultivated under artificial light with a specific wavelength range. [Solution] The soapwort of the present invention is cultivated by irradiating it with artificial light having a specific wavelength range, and the extract exhibits excellent collagen production promoting effect, MMP inhibitory effect, hyaluronic acid production promoting effect, cell proliferation promoting effect, and antioxidant effect. Furthermore, topical or internal skin preparations containing these effects are particularly effective and also exhibit excellent safety and stability. The soapwort extract of the present invention can be used not only in the field of beauty, such as preventing skin aging, but also in the field of medicine, such as suppressing functional decline due to aging, and is expected to be applied to cosmetics, foods, quasi-drugs, and pharmaceuticals.

The invention discloses an aryl oxadiazole compound with a chemical structural formula as shown in the specification or pharmaceutically acceptable salt thereof. In-vitro experiment results show that the compound has a remarkable inhibition effect on DENV, the therapeutic index (TI) of the compound is far higher than that of a clinical reference substance ribavirin, the TI value of a preferred compound such as I-29 exceeds 1131.86, and the TI value of the preferred compound is far higher than that of the clinical reference substance ribavirin. The characteristics of high efficiency and low toxicity are highlighted. In addition, the preparation method is simple in process, high in yield, mild in reaction condition and suitable for large-scale production and clinical popularization.

This invention relates to the application of ALKBH5 as a target in the preparation of drugs for inhibiting the progression of TNBC, and to the drugs themselves. This application discovers mRNA m 6 The alpha-modifying demethylase ALKBH5 is specifically highly expressed in triple-negative breast cancer (TNC). Using spontaneous TNC models and xenograft tumor models, knockout or knockdown of ALKBH5 significantly inhibited breast hyperplasia and the development of TNC, and promoted tumor differentiation. Simultaneously, the specific inhibitor EN300-14040 of ALKBH5 significantly inhibited the growth of TNC organoids, promoted TNC cell differentiation, and enhanced the sensitivity of TNC organoids to the endocrine drug 4OH-T, exhibiting a synergistic inhibitory effect with 4OH-T. Therefore, ALKBH5 represents a potential novel therapeutic target for TNC, and ALKBH5 inhibitors are a potential new type of drug for the treatment of TNC.

The present invention relates to a compound having an inhibitory effect on a plurality of sodium ion channels, or a pharmaceutically acceptable derivative thereof, a pharmaceutical composition comprising same, and a use thereof as a pan-sodium ion channel blocker.

The invention belongs to the technical field of medicines, and particularly relates to an aryl dicarboxylic acid compound, a preparation method and application of the aryl dicarboxylic acid compound as an antibacterial agent. The compound is shown as a formula (1), wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are independently selected from hydrogen and halogen. Two ends of the molecule are connected through an N-phenylpropanamide connecting arm, the molecule is a compound with a novel structure, and the series of compounds have a relatively strong inhibition effect on acinetobacter baumannii and are worthy of further research and development.

The application discloses application of undecyl-prodigiosin in inhibition of a root rot pathogen (Fusarium oxysporum) of Salvia miltiorrhiza, and belongs to the technical field of microbial pesticides. 25 H 33 The compound has a molecular formula of C 50 N3O, is derived from Streptomyces aurantiacus YS-4, has a concentration-dependent inhibitory effect on the Fusarium oxysporum, an EC of 33.1 μg / mL, and an inhibition rate of 83.3% at 400 μg / mL. The application further provides a preparation containing the compound, wherein the concentration of the compound is not less than 20 μg / mL, and the concentration of the target area after application is controlled in a range of 20 μg / mL to 400 μg / mL, so that the root rot of Salvia miltiorrhiza can be effectively prevented and treated. As a natural microbial metabolite, the compound is environment-friendly, has no residue, and is not easy to produce drug resistance, solves the pollution problem of chemical prevention and treatment, and provides a new scheme for green prevention and treatment of the root rot of Salvia miltiorrhiza.

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.

The invention belongs to the technical field of biology, and particularly relates to application of baicalin to preparation of a medicine for treating preeclampsia by inhibiting trophoblast ferroptosis induced by NETs. The baicalin inhibits downstream signal transduction by specifically interfering a key activation step of PKC [beta] 2 and a membrane translocation process coupled with a second signal, and finally plays a role in inhibiting ferroptosis of trophoblasts. The discovery provides a brand new perspective for understanding the molecular action mechanism of the medicine. According to the application, baicalin influences ferroptosis induced by NETs in trophoblast cells by inhibiting membrane translocation and activation of PKC beta2, so that the biological function of baicalin is exerted. The discovery of the mechanism further deepens the important significance of people on NETs and baicalin in disease induction and treatment, and a thought is provided for research and development of a new treatment scheme for preeclampsia.

The application discloses a kind of miraculin compounds and its extraction method and application, belong to the field of traditional Chinese medicine extraction, specifically related to a kind of miraculin compounds as shown in general formula (I) and (II) isolated from Rhododendron dauricum and the extraction method of the compound, and the compound or the isomer of the compound, or the inhibitory effect of the compound on inflammation in pharmaceutically acceptable salt or pharmaceutical composition comprising the compound can be used for preparing anti-inflammatory drugs.The application further enriches the structural diversity of active substances of Rhododendron dauricum, which lays a foundation for subsequent related biological activity tests of monomeric compounds, provides active lead compounds for new drug development, and also provides a theoretical basis for in-depth research and development of Rhododendron dauricum medicinal materials.

The invention relates to a triterpenoid saponin compound, a preparation method thereof and application of the triterpenoid saponin compound in preparation of anti-neuroinflammation drugs. The triterpenoid saponin compound has a structure as shown in a formula I. An in-vitro anti-neuroinflammation activity experiment proves that the triterpenoid saponin compound has an obvious inhibition effect on lipopolysaccharide (LPS)-induced BV2 cell inflammation, and can be used as a novel anti-neuroinflammation drug and a neurodegenerative disease treatment drug. Formula I

The application discloses a preparation method of ethanol extract of Drynaria Rhizome and application thereof. The method comprises the following steps: crushing and sieving Drynaria Rhizome, adding ethanol, reflux extraction, combining filtrates, vacuum concentration and drying, and thus the ethanol extract of Drynaria Rhizome is obtained. The in-vitro alpha-glucosidase enzyme inhibition experiment shows that the ethanol extract of Drynaria Rhizome has a significant inhibitory effect on alpha-glucosidase enzyme, and the IC 50 is about 142.68 μ g / mL. Therefore, the ethanol extract of Drynaria Rhizome can be used for preparing a hypoglycemic drug, health care product or functional food, and has a wide application prospect.

The invention discloses application of eupatolide in preparation of a medicine for preventing and treating inflammatory bowel disease, application of eupatolide in preparation of a medicine for preventing and treating inflammatory bowel disease and application of a medicine preparation containing eupatolide in preparation of a medicine for preventing and treating inflammatory bowel disease, and researches that eupatolide (EPT) can be used for preparing the medicine for preventing and treating inflammatory bowel disease through targeting pyruvate kinase isoenzyme 2 (PKM2, Gene ID: 5135). The inflammatory response, glycolysis metabolism and mitochondrial homeostasis are synergistically regulated and controlled, so that the inhibition effect on the inflammatory bowel disease is exerted. Meanwhile, EPT has the advantages of being low in dosage, feasible in oral administration, free of obvious toxic and side effects and the like, and a solid experimental basis is provided for further developing EPT into candidate drugs for preventing and treating inflammatory bowel diseases.

A series of sofalcone derivatives are provided.SOLUTION: A series of sofalcone derivatives provided by the present invention are, for example, compounds having a structure of formula (I), and have platelet aggregation inhibitory and antithrombotic effects. The sofalcone derivatives of the present invention are TxA2 receptor antagonists, have an inhibitory effect on platelet agglutination, and do not easily affect the hemostatic function. The present invention also provides a method for preparing the sofalcone derivative, and a method for using the sofalcone derivative for preventing or treating thrombotic diseases, or for inhibiting platelet aggregation.SELECTED DRAWING: None

A compound useful as an active ingredient in a pharmaceutical composition for the treatment of cancer related to the activation of immune cells or cancer resistant to treatment with anti-PD-1 / anti-PD-L1 antibodies is provided. The inventors hereof have conducted studies on a compound useful as an active ingredient in a pharmaceutical composition for the treatment of cancer related to the activation of immune cells or cancer resistant to treatment with anti-PD-1 / anti-PD-L1 antibodies and discovered that a pyridazinyl-thiazolcarboxamide compound has an inhibitory effect on DGKβ (DGKzeta), leading to the achievement of the present invention.The pyridazinyl-thiazolcarboxamide compound of the present invention has an inhibitory effect on DGK and can be used as a therapeutic agent for the treatment of cancer related to the activation of immune cells or cancer that offers resistance to treatment with anti-PD-1 antibodies / anti-PD-L1 antibodies.

The invention discloses a phenoxazine skeleton-containing drug small molecule and application thereof, and belongs to the technical field of synthesis of heterocyclic compounds and antitumor drugs, the phenoxazine skeleton-containing drug small molecule has an inhibition effect on HepG2 and A549, a phenoxazine derivative 7c with the third site connected with a methoxy group at the tail end of a phenoxazine structure benzene ring has a better overall effect, and the phenoxazine skeleton-containing drug small molecule can be applied to preparation of antitumor drugs. The inhibition rates of the compound on HepG2 and A549 are respectively 87.67% and 94.23%. 7g of the phenoxazine derivative of which the methyl ester structure is connected to the third site of the phenoxazine structure only has an obvious effect on A549, and the inhibition rate in A549 cells is 96.00%.