Application of betulinic acid derivatives in preparation of anti-liver lesion medicines

A technology of betulinic acid and derivatives, which is applied in the field of medicine, can solve the problems of lack of active groups in the mother nucleus, difficulty in preparing derivatives, special structure of pentacyclic triterpenoids, etc., and achieves wide application and good anti-hepatic fibrosis The effect of chemical activity

Active Publication Date: 2020-12-04
NANTONG UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are few reports on the anti-hepatic fibrosis effect of betulinic acid and its derivatives, and the pentacyclic triterpenoids have a special structure, the mother

Method used

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  • Application of betulinic acid derivatives in preparation of anti-liver lesion medicines
  • Application of betulinic acid derivatives in preparation of anti-liver lesion medicines
  • Application of betulinic acid derivatives in preparation of anti-liver lesion medicines

Examples

Experimental program
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Effect test

Embodiment 1

[0021] Embodiment 1, structural formula is the preparation of the compound of formula I-formula VI

[0022] The invention adopts a microbial transformation method, uses betulinic 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.

[0023] Taking Circinella muscae CGMCC 3.2695 as an example, the process of preparing the compound whose structural formula is formula I-formula VI is as follows:

[0024] 1) Fermentation, transformation and extraction

[0025] 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 ...

Embodiment 2

[0032] Example 2 Anti-hepatic fibrosis activity of compound I, compound II, compound III, compound IV, compound V and compound VI of the present invention

[0033] 1) Experimental materials

[0034] Instruments and reagents: CO 2 Incubator (Jouan IGO150); Microplate reader (Bio-TEK ELx800); Fluorescence inverted microscope (Olympus IX51); MTT cell proliferation and cytotoxicity detection kit (Biotech Institute), RPMI 1640 medium (Gibcol BRL ), RNase A, fetal bovine serum, dimethyl sulfoxide (DMSO), trypsin (Shanghai Bioengineering Co., Ltd.).

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PUM

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Abstract

The invention belongs to the field of medicines, and discloses betulinic acid derivatives or pharmaceutically acceptable salts thereof, and application of the betulinic acid derivatives or pharmaceutically acceptable salts thereof in preparation of anti-liver lesion medicines. The betulinic acid is successfully subjected to structural modification by a microbial conversion technology, a pluralityof novel compounds are obtained, and in-vitro anti-hepatic fibrosis cell tests prove that the compounds have better anti-hepatic fibrosis activity, can be used as active ingredients of anti-hepatic fibrosis medicines and have wide application.

Description

technical field [0001] The invention relates to the field of medicine, in particular to the application of betulinic acid derivatives in the preparation of anti-hepatopathy drugs. Background technique [0002] Hepatic fibrosis is caused by various pathogenic factors leading to liver injury. Hepatic stellate cells are activated to become myofibroblast-like cells with a strong ability to generate extracellular matrix, and then the production of collagenase inhibitors increases and collagenase activity decreases. , so that the ratio between the production and degradation of extracellular matrix in the liver is out of balance, which eventually leads to the excessive deposition of liver collagen and liver fibrosis. Liver fibrosis continues to deteriorate and lead to liver cirrhosis and even liver cancer, so the chain of "hepatitis-hepatic fibrosis-liver cirrhosis-liver cancer" is recognized as a common path for various chronic liver diseases to lead to serious consequences. Stud...

Claims

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Application Information

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IPC IPC(8): A61K31/56A61P1/16A61P35/00C07J63/00C12P33/12C12P33/06C12P33/02C12R1/645
CPCA61K31/56A61P1/16A61P35/00C07J63/008C12P33/02C12P33/06C12P33/12A61K2300/00
Inventor 陈广通储呈娇朱洺娴宋开南宋妍
Owner NANTONG UNIVERSITY
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