1683 results about "Inhibitory effect" patented technology

The invention relates to the field of medicinal chemistry, in particular to a substituted quinolinone compound targeting KRASG12D and application of the substituted quinolinone compound. Pharmacological tests prove that the affinity effect of the synthesized compound on a KRASG12D mutant is superior to that of a lead compound KAL-21404358. The compounds WY1-014 and WY1-062 have ideal inhibition effects on cells of human lung cancer (A549), human melanoma (A375) and human colon cancer (LOVO). The compound WY1-062 has excellent anti-tumor activity, and the activity of the compound WY1-062 is superior to that of cis-platinum.

The invention relates to the field of medicinal chemistry, relates to a general KRAS inhibitor and medical application thereof, and particularly relates to a compound targeting KRAS and mutants KRASG12C and KRASG12D thereof and medical application of the compound. The pharmacological test result of the affinity of KRAS and mutants thereof shows that the affinity of the compound to a KRAS wild type and a KRASG12C mutant type thereof and a KRASG12D mutant type thereof is superior to that of a lead compound, and the compound has a potential inhibition effect on target spots of the KRAS wild type and the KRASG12C mutant type thereof and the KRASG12D mutant type thereof.

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 present invention provides a compound as shown in formula (I), and a pharmaceutically acceptable salt of the compound. The compound in the present invention exhibits a strong inhibitory effect on Lp(a) assembly, and can be used for treating cardiovascular diseases (CVD).

A compound as an LPAR1 antagonist, a pharmaceutical composition thereof and a use thereof. A compound represented by formula (I), as well as a racemate, stereoisomer, tautomer, nitrogen oxide, or pharmaceutically acceptable salt thereof. The compound of the LPAR1 antagonist has a good inhibitory effect on LPAR1, has excellent pharmacokinetic properties, and has good druggability.

The invention belongs to the technical field of organic chemical synthesis, and particularly relates to a gentiopicroside amide derivative, a synthesis method and application. A series of gentiopicroside amide derivatives are synthesized by taking gentiopicroside as a research object, carrying out structural modification on 6 '-site hydroxyl of gentiopicroside and introducing a benzoyl chloride group into a gentiopicroside structure. The synthetic method has the beneficial effects that on one hand, the synthetic method of the gentiopicroside amide derivative, which is mild in reaction condition and environment-friendly, is established; on the other hand, the 20 synthesized gentiopicroside amide derivatives have a remarkable inhibition effect on expression of LPS-induced THP-1 macrophage IL-6 and STAT3 protein content, the anti-inflammatory activity is remarkable, the action effect is superior to that of parent compound gentiopicroside, and a new thought is provided for preparation of STAT3 small-molecule inhibitors and anti-inflammatory drugs.

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.

Disclosed are compounds having PTPN2 inhibitory effects and a use thereof. Specifically, disclosed are a class of compounds having protein tyrosine phosphatase inhibitory effects or pharmaceutically acceptable salts thereof, as well as a use thereof for treating and / or preventing diseases or conditions related to abnormal expression of protein tyrosine phosphatase. The compounds are represented by formula (I).

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 relates to a preparation method of an effective part extract of n-butyl alcohol of Eupatorium chinense and application of the effective part extract in treatment of diabetes complicated with depression. The technical scheme of the invention is to provide an extract of the n-butyl alcohol effective part of the eupatorium chinense, which can be used for treating diabetes complicated by depression diseases. In-vitro experiments show that the eupatorium chinense extract has an inhibition effect on acetylcholin esterase (AChE). In-vivo animal experiments find that classical anti-diabetes and depression treatment drugs, namely metformin hydrochloride and fluoxetine hydrochloride, are taken as positive controls, experimental research on the treatment effect of the effective part extract of the n-butyl alcohol of the eupatorium chinense on mice suffering from diabetes complicated with depression is developed, and research results show that the extract can regulate insulin resistance and can be used for treating diabetes complicated with depression. The glycometabolism of mice with diabetes mellitus complicated with depression is improved, and the depression symptom is improved. The extract has a remarkable effect of treating diabetes mellitus complicated with depression, has a good effect of treating diabetes mellitus complicated with depression, and is expected to be developed into a new natural medicine for treating diabetes mellitus complicated with depression.

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 invention belongs to the field of anti-cancer metal complexes, and particularly relates to a copper complex with anti-cancer activity and a preparation method and application thereof. Cu (OAc) 2H2O and coumarin-3-formyl-(2-aminomethylpyridine) are respectively dissolved in a solvent, the two solutions are mixed and stirred at room temperature to react for a period of time, the reaction solution is filtered, the filtrate is sealed and naturally volatilized at room temperature for 3-7 days, the complex can be obtained, the IC50 value of the complex to Hela cervical cancer cells is 0.8964 + / -0.09 mu M, and the IC50 value of the complex to Hela cervical cancer cells is 0.8964 + / -0.09 mu M. According to the present invention, the inhibition effect of the complex on HeLa cervical cancer cells is 3.38 times of the inhibition effect of cis-platinum, the toxicity of the complex on normal cells but HUVEC is very small, IC50 is greater than 100 [mu] M, and the complex has a high selectivity coefficient SI (SI = normal cell IC50 / cancer cell IC50), and the selectivity coefficient SI is greater than 111 and is 584 times of the selectivity coefficient of cis-platinum (SI = 0.19). The complex has the capability of inducing apoptosis of cancer cells and has concentration dependence. Meanwhile, the complex can retard cancer cells and an S phase so as to inhibit cell proliferation, and can generate an intercalation effect with HS-DNA (High-Speed Deoxyribose Nucleic Acid).

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 invention relates to an anti-cryptosporidium micromolecular lead compound of a target cryptosporidium helicase. Comprising the following steps: S1, detecting enzyme activity parameters of a drug target helicase (CpeIF4A) and an inhibition effect of Roc-A on the drug target helicase: expressing and purifying a CpeIF4A recombinant protein containing an MBP tag; detecting the enzyme activity; detecting the inhibition effect of the Roc-A on the enzyme activity; determining the affinity between the Roc-A and the CpeIF4A through a heat transfer experiment; s2, in-vitro drug effect determination: evaluating the direct killing capability of Roc-A on sporozoites; the inhibition effect of Roc-A on cryptosporidium is determined through an in-vitro cell infection model, an EC50 value is obtained, and the intracellular period of the Roc-A mainly playing the inhibition effect is determined; detecting the toxicity of Roc-A to host cells to obtain a TC5 value), and obtaining an in-vitro insect-resistant selectivity index (SI); and S3, in-vivo drug effect test: establishing a C57BL / 6IFN-gamma gene knockout mouse infection model to evaluate the effectiveness and safety of Roc-A. The invention determines that the Roc-A has the potential of being further developed into the cryptosporidium-resistant drug, and verifies that the targeted eIF4A can resist cryptosporidium infection.

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 provides an aromatic fused ring compound, a pharmaceutical composition containing the compound and application of the aromatic fused ring compound, and relates to the technical field of medicines. The aromatic fused ring compound disclosed by the invention has a structure as shown in a formula (I): # imgabs0 # or a stereoisomer and pharmaceutically acceptable salt thereof, wherein the structural unit # imgabs1 # is selected from # imgabs2 # or # imgabs3 #, and each substituent group is defined in the specification. The aromatic fused ring compound has a strong inhibition effect on SIKs enzyme activity, has a positive regulation effect on TNF-alpha and IL-10 in serum of mice with acute inflammation, has a longer half-life period and a higher oral exposure amount, has a remarkable inhibition effect on NF-kappa B gene expression of THP-1 cells under MDP stimulation, and can be used for preparing medicines for treating acute inflammation. The traditional Chinese medicine composition has a remarkable weight recovery promoting effect on cachexia induced by cis-platinum.

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 mussel byssus polypeptide with antibacterial performance and application thereof.The mussel byssus polypeptide has an obvious inhibiting effect on gram-positive bacteria and gram-negative bacteria, can inhibit formation of biological membranes of the gram-positive bacteria and the gram-negative bacteria, shows different antibacterial activities on multiple drug-resistant bacteria, and has the advantages that the mussel byssus polypeptide can be used for preparing a drug-resistant agent; and the hydrogel has low cytotoxicity and good biocompatibility, and shows good adhesion capability. The polypeptide is short in peptide chain and small in molecular weight, is a micromolecular polypeptide with great value, shows wide application potential in multiple fields, and has important value in the fields of medicine preparation, medical equipment and daily chemical products.

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.

The invention provides a traditional Chinese medicine preparation for treating or improving depression, and relates to the technical field of traditional Chinese medicine pharmacy. The traditional Chinese medicine preparation is prepared from the following ten medicinal materials: semen aesculi, fructus citri, fructus toosendan, semen celosiae, herba commelinae, herba senecionis scandentis, fructus liquidambaris, semen pruni, common fenugreek seed and liquorice root, and all the medicinal materials are combined to achieve the effects of soothing liver and regulating qi, clearing liver and purging fire, regulating liver and spleen simultaneously, dredging meridians and collaterals and warming kidney yang, so that liver depression can be relieved, qi activity can be smooth, liver fire can be cleared and depression syndrome can be removed. The traditional Chinese medicine preparation disclosed by the invention has a remarkable improvement effect on depression-like behaviors of mice with depression and has a remarkable inhibition effect on neuroinflammation. Meanwhile, the traditional Chinese medicine preparation is combined with western medicines to treat depression, the effect is remarkable, the HAMD-17, HAMA and TESS scores of treated depression patients can be remarkably reduced, depression and anxiety moods of the patients are remarkably improved, adverse reactions are relieved, and the traditional Chinese medicine preparation provides a new thought for treating depression through traditional Chinese medicine.

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.