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Application of betulin and its derivatives in drugs with anti-hepatic fibrosis

An anti-hepatic fibrosis and liver fibrosis technology, applied in the field of medicine, can solve the problems of lack of active groups, special structure, and few reaction sites in the mother nucleus

Active Publication Date: 2021-05-18
NANTONG UNIVERSITY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, pentacyclic triterpenoids have a special structure, lack of active groups in the mother nucleus, and few reaction sites, so it is difficult to prepare derivatives that meet the requirements by conventional chemical reaction methods

Method used

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  • Application of betulin and its derivatives in drugs with anti-hepatic fibrosis
  • Application of betulin and its derivatives in drugs with anti-hepatic fibrosis
  • Application of betulin and its derivatives in drugs with anti-hepatic fibrosis

Examples

Experimental program
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Effect test

Embodiment 1

[0023]Example 1 Preparation of Compounds of Structure 1-9

[0024]The present invention employs a microbial conversion method, and the compound of the present invention is prepared by fermentation, extraction, separation, and the like by fermentation, extraction, separation. The strains of Muxiang (Mucor) can be purchased from the Microbial Squirite Preservation Management Center (CGMCC) of the Chinese Academy of Sciences, and the potato medium is selected from the solid beveled medium to 4 ° C.

[0025]The process of preparing a compound of the formula 1-9 is as follows: Total Multi Merrat Mucor Racemosus AS 3.205.

[0026](1) Fermentation, conversion, and extraction

[0027]The total Merrum Mucor Racemosus AS 3.205 is connected to 2 250 ml of triangular bottles (with 100 ml of potato medium) as seed fluid. After 1 day in shake bed, 26 ° C was increasing for 1 day, the growth of the bacterium was in a strong period, and 1 ml of seed fluid was taken up with a sterile pipette, and added to 20 10...

Embodiment 2

[0035]Example 2 Anti-liver fibrosis of the compound 1-9 of the present invention

[0036](1) Experimental materials

[0037]Instrument and reagents: CO2Culture Box (Jouan IGO150); enzyme symbol (Bio-Tek Elx800); fluorescence inverted microscope (Olympus IX51); MTT cell proliferation and cytotoxic test kit (Biyun Tian Biotechnology Research Institute), RPMI 1640 medium (Gibcol BRL ), RNasea, fetal bovine serum, dimethyl sulfoxide (DMSO), trypsin (Shanghai Bioengineering Co., Ltd.).

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Abstract

The invention discloses a class of betulin derivatives or their pharmaceutically acceptable salts and their application in the preparation of anti-hepatic fibrosis drugs. The present invention utilizes microbial transformation technology to successfully modify the structure of betulin and obtain a number of novel compounds. The in vitro anti-hepatic fibrosis cell test proves that these compounds have good anti-hepatic fibrosis activity and can be used as anti-hepatic fibrosis Active ingredient of fibrosis drug, has a wide range of uses.

Description

Technical field[0001]The present invention relates to the field of medicine, and more particularly to the use of birch alcohol derivatives in preparing applications with anti-liver fibrosis, more particularly to birch derivatives in preparing prevention and treatment of liver fibrosis.Background technique[0002]Hepatic fibrosis is a variety of pathogenic factors leading to liver injury, and hepatic star cells are activated to become a muscle fibroblasts having strong generation of extracellular matrix capabilities, which in turn increases the increase in collagenase inhibitory, and collagenase activity also declines. In order to imbalance between the generation and degradation between the liver extracellular matrix and the degradation, ultimate deposition of liver collagen is ultimately deposited into hepatic fibrosis. Hepatic fibrosis continues to deteriorate leading to cirrhosis or even liver cancer, so the chain of "hepatitis-hepatic fibrosis-cirrhosis-liver cancer" is recognized ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/56A61P1/16A61P35/00
CPCA61K31/56A61P1/16A61P35/00
Inventor 陈广通杨圣菊宋妍陈晨
Owner NANTONG UNIVERSITY