1311 results about "Inhibitory effect" patented technology

The present invention belongs to the technical field of medicinal chemistry, and particularly relates to a pyrimidine macrocyclic compound. The compound has a good inhibitory effect on KRAS mutations, has a good inhibitory effect on the G12V mutation and other types of mutations of the KRAS gene, can be used as a general KRAS inhibitor, and can be used for the treatment of tumors driven by KRASG12V and other types of gene mutations.

The present invention relates to a compound as shown in formula (A) having a pan-RAS inhibitory effect, or an isotopic derivative or stereoisomer thereof, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the compound, and the use of the compound of formula (A) in the prevention and / or treatment of cancers, tumors, inflammatory diseases, autoimmune diseases or immune-mediated diseases.

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 discloses a Trichoderma auritum GUWM22 strain and application thereof, and belongs to the field of microorganisms. The preservation number of the trichoderma auritum GUWM22 is CCTCC (China Center for Type Culture Collection) NO: M20242639, the preservation date is November 26, 2024, the preservation unit is China Center for Type Culture Collection, and the preservation address is Wuhan University, Wuhan, China. Experiments prove that the GUWM22 has a very strong inhibition effect on six pathogenic bacteria (phytophthora nicotianae, phytophthora capsici, botryosphaeria dothidea, alternaria alternata, phomopsis and colletotrichum capsici), the bacteriostasis rate reaches 78% or above, in addition, the GUWM22 also has a good prevention and treatment effect on anthracnose of picked peppers (line peppers), the prevention effect is 82.11%, and it can be seen that the GUWM22 can be used for preventing and treating anthracnose of the picked peppers (line peppers). The Trichoderma aureum GUWM22 is a new biocontrol Trichoderma strain with good potential. The invention provides a new strain resource and an environment-friendly and efficient biocontrol approach for effective prevention and treatment of pepper anthracnose.

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 relates to an amido-substituted aromatic heterocycle inhibitor as well as a preparation method and application thereof. Specifically, the compound disclosed by the invention has a structure as shown in a formula (I), and each group is defined in the specification. The invention further discloses a preparation method of the compound and application of the compound as a KRAS mutation inhibitor. The compound has a very good inhibition effect on KRAS mutation and has better pharmacodynamic and pharmacokinetic performance and lower toxic and side effects. # imgabs0 #

The present invention addresses the problem of providing an improving agent for improving a stratum corneum barrier function without external replenishment with any moisturizing substance and a pharmaceutical composition containing said improving agent. The present invention provides: a stratum corneum barrier function improving agent which contains a glycolytic inhibitor as an active ingredient; the stratum corneum barrier function improving agent in which the glycolytic inhibitor is at least one selected from the group consisting of a glucose transporter inhibitor and a glucose competitive inhibitor; either of said stratum corneum barrier function improving agents having at least one selected from the group consisting of an inhibitory effect on the loss of skin moisture retention capacity and an inhibitory effect on skin permeability enhancement; and a pharmaceutical composition which contains any of said stratum corneum barrier function improving agents.

The invention relates to the technical field of ferula asafoetida endophytic fungi separation and purification, in particular to alkaloid compounds in ferula asafoetida endophytic fungi as well as a preparation method and application of the alkaloid compounds in the ferula asafoetida endophytic fungi. And extracting with dichloromethane to obtain dichloromethane part extract, and purifying and separating the dichloromethane part extract by adopting silica gel column chromatography and high performance liquid chromatography to obtain the alkaloid compounds in the endophytic fungi of ferula sinkiangensis. The alkaloid compound in the ferula sinkiangensis endophytic fungi is disclosed for the first time, the compound is subjected to an in-vitro anti-tumor pharmacodynamic experiment, and according to the experiment result, the alkaloid compound has a certain inhibition effect on MCF-7 cells; therefore, the alkaloid compound can be used for preparing the medicine for preventing and treating the breast cancer, and a new medicine is provided for preventing and treating the breast cancer.

The invention provides a dual-targeting carrier material, a preparation method thereof and a preparation method of oleanolic acid nanoparticles wrapped by the dual-targeting carrier material, and belongs to the technical field of medicines. The oleanolic acid targeting nanoparticles are prepared by taking a dual-targeting high-molecular copolymer as a carrier material and adopting an emulsification-solvent evaporation method, so that the oleanolic acid can be protected from being quickly degraded, and the in-vivo circulation time of the oleanolic acid can be prolonged. Meanwhile, targeted delivery of oleanolic acid is realized through a targeted group, the concentration of the drug in tumor tissues is improved, and toxic and side effects on normal tissues are reduced. An MTT method is adopted, the inhibition effect of the oleanolic acid nanoparticles on cell growth is researched, and the result shows that the oleanolic acid targeting nanoparticles have a stronger effect of inhibiting tumor cell proliferation compared with an oleanolic acid raw material medicine.

The present invention discloses a broad-spectrum antibacterial peptide, and the amino acid sequence of the antibacterial peptide is GECEGNNRPVKKPQPRKKLPRFKKC-NH2. Based on melittin, the present invention designs antibacterial peptides by predicting based on a deep learning model, and obtains antibacterial peptides with broad-spectrum bacteriostasis, thermal stability and low hemolytic property, which have good inhibitory effects on skin pathogenic bacteria such as Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Candida albicans and Propionibacterium acnes. Peptides predicted as AMP amino acid sequences by the deep learning model antibacterial peptide prediction tool amPEPpy are selected for screening, and by using a biosynthesis technique, they are expressed, extracted and purified in Escherichia coli, reducing the workload and screening period of screening, and increasing the probability of screening out broad-spectrum and thermally stable biosynthetic antibacterial peptides.

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 a composite double-protein hypoglycemic peptide as well as a preparation method and application thereof, and belongs to the technical field of animal and plant source double-protein active peptides. The method comprises the following steps: performing computer simulation enzyme digestion and virtual screening by utilizing bioinformatics to determine a protein raw material and protease, performing enzymolysis on animal and plant double proteins (soybean protein and casein) serving as raw materials by adopting neutral protease, and performing separation, purification and structural identification, thereby obtaining the protein. The protein peptide fragment with high alpha-glucosidase inhibitory activity is obtained by virtually screening molecular docking, and the amino acid sequences of the protein peptide fragment are shown as SEQ ID No: 6, SEQ ID No: 9 and SEQ ID No: 24. The compound double-protein peptide sequence provided by the invention has an inhibiting effect on the activity of alpha-glucosidase, can be used for preventing and treating diabetes mellitus, and can be used for long-term health care or treatment of people with impaired glucose tolerance or diabetics as a functional food ingredient.

The invention discloses a grape seed source anti-inflammatory peptide, and belongs to the technical field of biological medicine. The amino acid sequence of the anti-inflammatory peptide is selected from any one of WGF, SHFGF, EGPFF, WAPR, SFYRAF, HFAFL, PGRF or FDSF. A BPS-induced RAW 264.7 mouse mononuclear macrophage inflammation model is established, and the eight synthetic peptides are found to significantly reduce the content level of NO in inflammatory cells and have an inhibition effect on secretion of inflammatory factors TNF-alpha and IL-6. A qRT-PCR (quantitative reverse transcription-polymerase chain reaction) experiment shows that the synthetic peptide can inhibit expression of mRNA (messenger Ribonucleic Acid) of p65, Tnf alpha, Il6, Il1b and Nos2, and can play an anti-inflammatory role by regulating and controlling an NF-kappa B signal channel. According to the method, the high-activity anti-inflammatory peptide is screened from the wine brewing byproduct grape seeds for the first time, and green and high-value utilization of the grape processing byproduct is realized.

A nitrogen-containing polycyclic fused ring compound of formula I, a pharmaceutical composition thereof, a preparation method therefor and use thereof are related to the field of medicinal chemistry. The compound can be used as a selective and effective RET inhibitor. It has strong inhibitory effect on the RET gatekeeper residue mutant RET V804M, RET solvent-front residue mutant RET G810R and other clinically relevant RET mutants, as well as RET wt. The compound can also inhibit the growth of TT cell line derived from thyroid cancer and Ba / F3 cells transformed with various RET mutants, and induce the death of TT cells.

The invention discloses a coumarin KRAS-G12C inhibitor as well as preparation and application of the coumarin KRAS-G12C inhibitor. The coumarin compound disclosed by the invention has a remarkable inhibition effect on non-small cell lung cancer cells (NCI-H23 and NCI-H358) with high expression of KRAS-G12C and pancreatic cancer cells (MIAPaCa-2), is particularly used for preparing medicines for treating and / or preventing non-small cell lung cancer and pancreatic cancer, and has a good prospect of development and application of antitumor medicines.

The invention relates to the technical field of biological control of plant diseases, in particular to application of a bacillus atrophaeus strain and a preparation thereof to control wheat gibberellic disease caused by gibberellic maize. The preservation number of the strain is CGMCC (China General Microbiological Culture Collection Center) No.29799, and the strain is classified and named as the bacillus atrophaeus strain HHQGTS13-1 (Bacillus atrophaeus HHQGTS13-1). The bacillus atrophaeus strain HHQGTS13-1 is wide in application range to natural environment conditions such as temperature and pH, and has the capability of antagonizing fusarium maydis when the temperature is 10-45 DEG C and the pH value is 4-10. The bacillus atrophaeus strain HHQGTS13-1 can be used for obviously inhibiting the growth of fusarium maydis hyphae and enabling the hyphae to be deformed; the antagonistic bacillus HHQGTS13-1 strain has an obvious inhibition effect on spore germination of fusarium maydis, the spore germination inhibition rate is 97.10%, the prevention and treatment effect of the antagonistic bacillus HHQGTS13-1 strain fermentation liquor after wheat is inoculated with fusarium maydis pathogenic bacteria is 63.43%, and the antagonistic bacillus HHQGTS13-1 strain has good potential of preventing and treating plant diseases caused by fusarium maydis.

The invention relates to talaromyces cordiformis and application thereof. The talaromyces sp. Strain Dz-1118 is found to have an antagonistic inhibition effect on fusarium solani, fusarium oxysporum, fusarium pseudograminearum, fusarium verticillium, fusarium graminearum or botrytis cinerea, so that the talaromyces sp. Strain Dz-1118 can be used for preventing and treating root rot, fusarium wilt, stem rot, spike rot, gibberellic disease or gray mold.

The invention discloses a traditional Chinese medicine composition for resisting giant frog blue eye disease pathogen Elizabeth mileli and application of the traditional Chinese medicine composition, and relates to the technical field of aquaculture disease prevention and treatment. It is found for the first time that the radix scutellariae has a good effect of inhibiting the Elizabeth mille, and the herba houttuyniae does not have the effect of inhibiting the Elizabeth mille but can enhance the inhibiting effect of the radix scutellariae on the Elizabeth mille, that is, the herba houttuyniae has a synergistic enhancement effect; the traditional Chinese medicine composition of the radix scutellariae and the herba houttuyniae is expected to be applied to treatment of the blue eye disease of the giant spiny frog, and the Chinese herbal medicine composition is used for replacing antibiotics in the breeding process.

The invention relates to a preparation method and application of a metal ion type lipid nanoparticle delivery system for regulating mRNA transfection. The method comprises the following steps: (1) mixing mRNA and metal ions in a solvent for 5-15 minutes to obtain a mixture solution (water phase); and (2) blowing, beating and mixing the nanoparticle-containing solvent obtained in the step (1) and a lipid solvent, and wrapping the mixture in the water phase with lipid nanoparticles to obtain the metal ion type lipid nanoparticle delivery system for regulating mRNA transfection. The preparation method has the characteristics of mild preparation conditions and simple preparation steps. According to the application, the organ specific transfection capacity of a lipid nanoparticle delivery system containing different metal ions is verified through mouse experiments. An in-vitro imaging result shows that the system has an enhancement or inhibition effect on mRNA transfection in different organs. The discovery provides a reference basis for metal ion selection for clinically and accurately regulating mRNA in-vivo transfection, and has an important guiding value.

The invention relates to the technical field of biomedicine, in particular to application of gastrodin in prevention and treatment of Alzheimer's disease. The invention provides application of gastrodin in prevention and treatment of the Alzheimer's disease, and provides a new way for preventing and treating the Alzheimer's disease. And gastrodin is from gastrodia elata, is used as a mild medicinal and edible raw material component, and has no toxic or side effect on the body. Gastrodin is adopted as a raw material, and a series of experimental studies prove that gastrodin has an inhibitory effect on GSK-3beta / P38MAPK, and can obviously improve various pathological changes of the Alzheimer's disease caused by APOE4. The invention verifies the effect of gastrodin on the Alzheimer's disease high-risk factor APOE4, and provides a brand-new technical scheme and theoretical basis for developing medicines, health-care foods or nutritional supplements which take gastrodin as a core component and are used for preventing or treating Alzheimer's disease.

The invention relates to the technical field of biological medicine, in particular to application of a combination of a Cd1 and Mdr1 double-target inhibitor and an azole drug in preparation of an antifungal drug. Based on the fact that the compound as shown in the formula (I) can be used as a CCd1 and Mdr1 double-target inhibitor, the inhibition effect of the compound on candida albicans, candida auricula, candida glabrata, candida tropicalis, trichophyton rubrum and trichophyton indicus when the compound is combined with azole drugs is further evaluated, and the result shows that the compound as shown in the formula (I) has no obvious antibacterial activity on various fungi, and can be used for preparing a medicine for treating various fungi. The drug resistance of CCd1 and Mdr1 overexpression drug-resistant fungi can be reversed, the activity of Candida albicans, Candida auricula, Candida glabrata, Candida tropicalis, Trichophyton rubrum and Trichophyton indicus can be synergistically inhibited when the drug is combined with azole drugs, the treatment dosage of the azole drugs is effectively reduced, and the drug toxicity is small. Therefore, the compound shown in the formula (I) can improve the antifungal effect of azole drugs and reduce the drug resistance of the azole drugs.

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 discloses nematode-killing streptomyces JXSY860 and application thereof, and belongs to the technical field of microbial pesticides. According to the invention, a new strain of Streptomyces turiscabs JXSY860 is found, the new strain of Streptomyces turiscabs JXSY860 has been preserved in Guangdong Microbial Culture Collection Center on August 8, 2024, and the preservation number is GDMCC No: 64998. The invention also discloses a preparation method of the Streptomyces turiscabs JXSY860. Through verification, the JXSY860 strain provided by the invention has stronger lethal activity on second-stage larvae of root-knot nematode, has stronger inhibition effect on incubation of root-knot nematode eggs, has important application value on prevention and control of root-knot nematode diseases of crops, and can be widely applied to preparation of biological agents for preventing and controlling the root-knot nematode diseases.

The invention discloses a tripterine-sophocarpidine self-assembled nanoparticle and application thereof in preparation of an anti-tumor drug, and belongs to the field of biological medicine. The nanoparticles are formed by self-assembly of the tripterine and the sophocarpidine through supramolecular interaction, the molar ratio of the tripterine to the sophocarpidine is 1: 1-1: 3, and the self-assembly system effectively solves the problems of low Cst solubility, poor bioavailability, rapid in-vivo removal and the like; the inhibition effect on triple negative breast cancer (TNBC) is remarkably enhanced through the synergistic effect of Cst and Mar, and a new strategy is provided for expanding the application of a traditional Chinese medicine carrier-free self-assembly nano drug delivery system in the anti-tumor field.

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.

The invention provides a rehmannia fermented extract, a composition as well as a preparation method and application of the rehmannia fermented extract and the composition, and belongs to the technical field of biological medicines. According to the invention, raw dark green tea and rehmannia are fermented by using a single strain of eurotium cristatum to respectively obtain a raw dark green tea fermentation extract and a rehmannia fermentation extract. Experiments prove that the two extracts have a relatively good inhibition effect on dipeptidyl peptidase-4 when being independently used; furthermore, the two extracts are combined, and animal experiments prove that the composition has relatively good inhibitory activity on intestinal tract and excrement dipeptidyl peptidase-4 and also has a hypoglycemic effect.

The invention discloses a pharmaceutical composition for resisting tumors, and belongs to the field of medical biology. The STING antagonist can be used in combination with chemotherapy drugs to enhance the inhibition effect on tumors, the endoplasmic reticulum stress inducer can also be used in combination with chemotherapy drugs to achieve a better inhibition effect on tumors, and a good tumor inhibition effect is achieved in vivo and in vitro by combining chemotherapy, STING inhibition and endoplasmic reticulum stress treatment schemes. The invention provides a new medication idea for tumor treatment.

The present invention belongs to the field of traditional Chinese medicines, and particularly relates to Leixihaokang, a preparation method therefor, and use thereof. The Leixihaokang of the present invention is prepared from the following active pharmaceutical ingredients in parts by weight: 10 parts of Tripterygium glycosides and 0.1-1.3 parts of Artemisia annua extract. According to the present invention, animal experiments prove that the Leixihaokang can ameliorate renal damage in nephrotic syndrome caused by adriamycin, reduce the occurrence of proteinuria, and reduce the apoptosis of renal tissue cells. Meanwhile, the Leixihaokang of the present invention has a good inhibitory effect on renal, hepatic, splenic, and cardiac toxicity in the treatment process of nephrotic syndrome. According to the present invention, animal experiments also prove that the Leixihaokang can ameliorate skin injury in imiquimod-induced psoriasis, reduce inflammatory infiltration and alleviate skin damage. Meanwhile, the Leixihaokang has a certain degree of inhibitory effect on the hepatic and reproductive system toxicity in the treatment process of psoriasis.

The present invention provides an SLC6A19 inhibitor compound, a pharmaceutical composition, a preparation method, and a use. The compound has a good SLC6A19 inhibitory effect, and is used for the treatment of SLC6A19-mediated disorders and / or diseases, such as phenylketonuria, and the preparation of drugs for such disorders or diseases.

The invention discloses a whitening and freckle-removing composition, a conditioner, a medicine and a cosmetic. The whitening and freckle-removing composition is prepared from emblic leafflower fruit, passion fruit and Chinese ladiestresses root and leaf A; the phyllanthus emblica comprises a phyllanthus emblica raw material and / or a phyllanthus emblica extract, and the passion fruit comprises a passion fruit raw material and / or a passion fruit extract. Through scientific compatibility of the Chinese ladiestresses root-ginseng A and the second active component comprising one or more of the emblic leafflower fruit, the passion fruit and the salvia officinalis, the Chinese ladiestresses root-ginseng A has a remarkable inhibition effect on tyrosinase activity, can inhibit expression and functions of rate-limiting enzyme TYR in the melanin synthesis process, has a remarkable whitening and freckle-removing active effect, and has a remarkable whitening and freckle-removing effect. The composition is safe and efficient, and can be applied to various conditioners, medicines and cosmetics.