10 results about "Hederagenin" patented technology

The invention provides an application of hederagenin in preparation of a medicine used as an SKP2 degradation agent, and particularly provides an application of hederagenin in preparation of a medicine used as an SKP2 degradation agent. The invention also provides a PROTAC compound, which comprises a target protein POI ligand, an E3 ubiquitin ligase ligand and a linking chain Linker, the general formula of the ligand-Linker-E3 ligase ligand is as follows: a POI ligand-Linker-E3 ligase ligand. The invention also provides a preparation method and application of the PROTAC compound. The PROTAC design based on HED improves the tumor tissue targeting property, and shows low toxicity in an in-vivo experiment. The invention provides a novel SKP2 (SKP2) degradation agent. The degradation agent is expected to be capable of efficiently inducing ubiquitination degradation of SKP2 protein, and a treatment strategy with higher potential and clinical application prospect is provided for overcoming the limitation of the prior art by enhancing the specific killing capability on SKP2 high-expression tumor cells and verifying the remarkable tumor inhibition effect and good safety of the degradation agent in an animal model.

The invention discloses a novel application of hederagenin in preparation of a medicine for maintaining the dryness of alveolar II epithelial cells, the hederagenin is definitely used for preparing the medicine for maintaining the dryness of the alveolar II epithelial cells for the first time, and the repairing effect of the hederagenin on ATII dry damage is verified through in-vivo and in-vitro experiments. A brand new treatment strategy is provided for lung diseases such as acute lung injury, pulmonary fibrosis and the like which are characterized by ATII dry failure, the technical blank of intervention of natural active ingredients in ATII dry is filled up, a new way which is efficient, low in cost and easy to obtain is provided for ATII dry maintenance, the concentration of a medicine prepared from the natural active ingredients is screened, and the clinical application prospect is wide. An important theoretical basis is provided for further medication and medicine preparation, meanwhile, the pharmacological application range of the hederagenin is expanded, and a new target and a new strategy are provided for subsequent intervention treatment of lung diseases such as acute lung injury and pulmonary fibrosis needing injury repair.

The application relates to the technical field of biological medicine, and discloses a preparation method of a hederosapogenin STING channel inhibitor, which comprises the following steps: taking appropriate hederosapogenin and aromatic compounds, adding N,N-dimethylformamide as a reaction solvent, and adding appropriate K2CO3; stirring under a heating reflux state for a certain time, monitoring the reaction process through thin layer chromatography until the reaction is completed; after the reaction is completed, the N,N-dimethylformamide is evaporated under reduced pressure, the obtained residue is dissolved in dichloromethane, and the residue is extracted and washed with deionized water and saturated brine in sequence; the organic layer is collected, dried with anhydrous sodium sulfate, filtered, evaporated under reduced pressure, and a crude product is obtained; the crude product is separated and purified through a silica gel column chromatography, and a target compound, namely a STING channel inhibitor derivative, is obtained. The hederosapogenin is chemically modified to synthesize a derivative with high STING channel activity, which is used for treating immune and inflammation related diseases.

The invention provides a medicine containing hederagenin and application of the medicine in regulating and controlling lysozyme to block gastritis-cancer transformation, the interaction relation between hederagenin and a key target spot is preliminarily determined by combining the key target spot LYZ of gastric inflammation-cancer screened by early-stage bioinformatics and applying a molecular docking technology, and then verification is performed by applying in-vivo and in-vitro experiments. Results of research discover that the common component hederagenin of astragalus membranaceus-curcuma zedoary and the key target LYZ of the gastric inflammation-cancer have an interaction relationship, and in-vivo and in-vitro experiments prove that the hederagenin can regulate and control the key target LYZ of the gastric inflammation-cancer, so that a new foundation is laid for further screening of core medicine components and optimization of traditional Chinese medicine formulas. The research and development of effective drugs for preventing and treating early gastric cancer have important significance.

The invention discloses a hederagenin C-2 heterocyclic oxime ester derivative as well as a preparation method and application thereof, and belongs to the technical field of organic chemistry. The structure of the derivative is shown in the specification, and in the formula, R represents furan, thiazole, oxazole, thiophene or 2, 3-dimethoxybenzene. Pharmacological tests show that the hederagenin C-2 heterocyclic oxime ester derivatives (H3W-FN, H3W-SZ, H3W-EZ, H3W-SF and H3W-OB) prepared by the invention all have MDR reversal activity, and part of the hederagenin C-2 heterocyclic oxime ester derivatives (H3W-SZ) have better MDR reversal activity than verapamil, so that the sensitivity (plt; 0.01), is a P-gp inhibitor with more excellent MDR reverse activity, and can be combined with common antitumor drugs to exert good antitumor activity.

The present invention belongs to the technical field of pharmaceuticals. Disclosed are a pharmaceutical composition for treating a TDP-43 proteinopathy, and a preparation method therefor and the use thereof. The pharmaceutical composition comprises at least one of each of compounds of class A and compounds of class B. The compounds of class A comprise at least one of sodium aescinate, a sodium aescinate derivative, hederagenin or a hederagenin derivative; and the compounds of class B comprise at least one of dehydrated icaritin, a dehydrated icaritin derivative, diosmin or a diosmin derivative. The pharmaceutical composition has a good therapeutic effect on the TDP-43 proteinopathy.

The invention discloses a hederagenin C-23 heterocyclic ester derivative as well as a preparation method and application thereof, and belongs to the technical field of organic chemistry. The structure of the derivative is shown in the specification, wherein R represents pyrazole, thiazole, oxazole, furan, pyrimidine, pyrazine or indole. Pharmacological tests show that part of hederagenin C-23 heterocyclic ester derivatives (T-BZ, T-SZ, T-EZ, T-MD and TBQ) prepared by the invention have better MDR reversal activity than verapamil, can significantly increase the sensitivity (p < 0.0001) of drug-resistant KBV cells to paclitaxel, are P-gp inhibitors with more excellent MDR reversal activity, can be used in combination with common antitumor drugs, and can be used for preparing drugs for treating tumors. The good anti-tumor activity is realized.

The present application belongs to the technical field of detection, and relates to a detection method for multiple active ingredients of Shishi Tonglin capsules, comprising simultaneously determining the contents of salvianolic acid B, protodioscin, dioscin, hederagenin and tanshinone II A in Shishi Tonglin capsules based on UPLC-QAMS method, or / and simultaneously determining the contents of salvianolic acid B, verbascoside, berberine hydrochloride, pachymic acid A and tanshinone II A in Shishi Tonglin capsules based on HPLC-QAMS method. The present application utilizes the method of combining liquid chromatography with one measurement multiple evaluation, determines one stable, easily obtained and low-priced active ingredient, calculates the contents of other ingredients by using the relative correction factor method, realizes the simultaneous determination of multiple ingredients in Shishi Tonglin capsules, and has the advantages of simple determination method, good accuracy of detection results and reduced detection cost.

The application discloses a process for affinity separation of active ingredients in Inonotus obliquus by using an extramembrane region of VEGFR2 and application thereof, and relates to the technical field of active ingredient extraction. Eight active ingredients, namely echinacoside, strophanthin, typhonioside, hederagenin, asiaticoside, lanosterol, betulinol and shionin, are selected to study the inhibiting effect of the active ingredients on cervical cancer cells. The detection liquid is taken to perform sodium dodecyl sulfate-polyacrylamide gel electrophoresis and Western blot analysis, the expression amount of VEGFR-2 related pathway proteins is determined, and the regulation effects of strophanthin, betulinol, hederagenin and lanosterol on the PI3K / AKT signal pathway, the PLC gamma / ERK signal pathway, Bad protein, Caspase-9 protein and Cleaved Caspase-9 protein of SiHa cells are studied.

The present invention belongs to the technical field of pharmaceuticals. Disclosed are a pharmaceutical composition for treating a TDP-43 proteinopathy, and a preparation method therefor and the use thereof. The pharmaceutical composition comprises at least one of each of compounds of class A and compounds of class B. The compounds of class A comprise at least one of sodium aescinate, a sodium aescinate derivative, hederagenin or a hederagenin derivative; and the compounds of class B comprise at least one of dehydrated icaritin, a dehydrated icaritin derivative, diosmin or a diosmin derivative. The pharmaceutical composition has a good therapeutic effect on the TDP-43 proteinopathy.