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Application of ursolic acid derivatives in the preparation of drugs for preventing or treating cardiovascular diseases

A technology of ursolic acid and derivatives, applied in the field of medicine, can solve the problems of lack of active groups in the mother nucleus, difficulty in obtaining derivatives, incomplete chemical and pharmacological research on ursolic acid derivatives, etc., and achieve good cardiomyocyte protection activity Effect

Active Publication Date: 2021-11-30
NANTONG UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the special structure of pentacyclic triterpenoids, the parent nucleus lacks active groups and few reaction sites, it is difficult to obtain derivatives with hydroxyl, carbonyl and other modifications on the parent nucleus by conventional chemical reaction methods
Therefore, the chemical and pharmacological studies of ursolic acid derivatives with structural modification of the core are not yet comprehensive

Method used

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  • Application of ursolic acid derivatives in the preparation of drugs for preventing or treating cardiovascular diseases
  • Application of ursolic acid derivatives in the preparation of drugs for preventing or treating cardiovascular diseases
  • Application of ursolic acid derivatives in the preparation of drugs for preventing or treating cardiovascular diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Embodiment 1 structural formula is the preparation of the compound of formula I-formula IV

[0019] The invention adopts a microbial conversion method, uses ursolic acid as a raw material, and undergoes steps such as fermentation, extraction, and separation to prepare the compound of the invention. Circinella genus strains can be purchased from the Chinese Academy of Sciences Microbial Culture Collection Center (CGMCC), using potato medium, and stored on a solid slant medium in a refrigerator at 4°C.

[0020] Taking Circinella muscae CGMCC 3.2695 as an example, the process of preparing the compound whose structural formula is formula I-Formula IV is as follows:

[0021] 1) Fermentation, transformation and extraction

[0022] Put Circinella muscae CGMCC 3.2695 into two 250mL Erlenmeyer flasks (containing 100mL potato culture medium) as seed solution. After shaking and culturing on a shaker at 160 rpm and 26°C for 1 day, when the mycelium growth is in a vigorous stage, ...

Embodiment 2

[0029] Example 2 Compounds Ⅰ-Ⅳ Protective Activity of Cardiomyocytes Damaged by Hydrogen Peroxide

[0030] (1) Experimental materials

[0031] CO 2 Incubator (Jouan IGO150); Microplate reader (Bio-TEK ELx800); Fluorescent inverted microscope (OlympusIX51); MTT cell proliferation and cytotoxicity detection kit (Biotech Institute), DMEM high glucose medium (Gibcol BRL ), fetal bovine serum, dimethyl sulfoxide (DMSO), trypsin (Shanghai Bioengineering Co., Ltd.), 30% hydrogen peroxide (H 2 o 2 ) (Tianjin Ruijinte Chemicals Co., Ltd.), H9c2 cells (Tumor Institute, Chinese Academy of Medical Sciences).

[0032] (2) Experimental method

[0033] The MTT method was used to determine the H of each test compound 2 o 2 Influence of damaged H9c2 cell viability: count the cells after digestion with trypsin, adjust the cell density of the cell suspension to 5×10 4 cells / mL, add 200 μL to each well of a 96-well culture plate, place in 5% CO 2 , 37°C constant temperature CO 2 Cultivat...

Embodiment 3

[0040] Example 3 Protective effect of compounds Ⅰ-Ⅳ of the present invention on cardiomyocyte ischemia-reperfusion injury

[0041] 1) Experimental materials

[0042] CO 2 Incubator (Jouan IGO150); Microplate reader (Bio-TEK ELx800); Fluorescent inverted microscope (OlympusIX51); MTT cell proliferation and cytotoxicity detection kit (Biotech Institute), DMEM high glucose medium (Gibcol BRL ), fetal bovine serum, dimethyl sulfoxide (DMSO), trypsin (Shanghai Bioengineering Co., Ltd.), H9c2 cells (Oncology Institute, Chinese Academy of Medical Sciences).

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Abstract

The invention belongs to the field of medicine, and discloses the application of a class of ursolic acid derivatives in the preparation of drugs for preventing or treating cardiovascular diseases. The present invention utilizes microbial transformation technology to successfully carry out structural modification to ursolic acid, and obtains 4 novel compounds with structural modification of the mother nucleus, which are confirmed by in vitro myocardial cell injury protection test and myocardial cell ischemia-reperfusion test. The compound has good cardiomyocyte protection activity, can be used as an active ingredient of drugs for treating myocardial infarction, coronary atherosclerotic heart disease, and chronic heart failure, and has wide applications.

Description

technical field [0001] The invention relates to the field of medicine, in particular to the application of ursolic acid derivatives in the preparation of drugs for preventing or treating cardiovascular diseases. Background technique [0002] With the improvement of living standards and population aging, and affected by social and environmental factors, the incidence of cardiovascular disease is increasing year by year, and it has become one of the diseases with the highest mortality in human beings. In the occurrence and development of various cardiovascular diseases such as myocardial infarction and ischemia-reperfusion injury, myocardial cell damage is often accompanied by cell apoptosis, which causes cardiovascular dysfunction. Myocardial ischemia and oxidative stress are important factors in the development of cardiovascular diseases. [0003] Ursolic acid, also known as ursolic acid, is a kind of pentacyclic triterpenes with special structure, which exists in many kind...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/56A61P9/00A61P9/04A61P9/10C12P33/06C12P33/02C07J63/00
CPCA61K31/56A61P9/00A61P9/04A61P9/10C07J63/008C12P33/02C12P33/06
Inventor 陈广通陆游佳张喆储呈娇宋开南宋妍
Owner NANTONG UNIVERSITY
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