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Application of cycloastragenol derivatives to preparation of medicament with anti-hepatic-fibrosis effect

A technology of cycloastragenol and liver fibrosis, applied in the field of medicine, can solve the problems of difficult preparation of derivatives, few reaction sites, lack of active groups, etc., and achieve good anti-hepatic fibrosis activity and wide application effect

Active Publication Date: 2018-12-14
义乌国信白蚁防治有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, cycloastragenol belongs to tetracyclic triterpenoids, lacks active groups, and has few reaction sites. It is difficult to prepare derivatives that meet the requirements by conventional chemical reaction methods.

Method used

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  • Application of cycloastragenol derivatives to preparation of medicament with anti-hepatic-fibrosis effect
  • Application of cycloastragenol derivatives to preparation of medicament with anti-hepatic-fibrosis effect
  • Application of cycloastragenol derivatives to preparation of medicament with anti-hepatic-fibrosis effect

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Embodiment 1, structural formula are the preparation of the compound of 1-6

[0023] The invention adopts a microbial conversion method, uses cycloastragenol as a raw material, and undergoes steps such as fermentation, extraction, and separation to prepare the compound of the invention. The strains of the genus Mucor can be purchased from the Chinese Academy of Sciences Microorganism Culture Collection Management Center (CGMCC), using potato culture medium, and storing them in a 4°C refrigerator on a solid slant medium.

[0024] Taking Mucor racemosus AS 3.20 as an example, the process for preparing compounds with structural formulas 1-6 is as follows:

[0025] 1) Fermentation, transformation and extraction

[0026] Put Mucor racemosus AS 3.20 into two 250mL Erlenmeyer flasks (containing 100mL potato 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, use a sterile pipette to...

Embodiment 2

[0035] Example 2 Anti-hepatic fibrosis activity of compound 1-6 of the present invention

[0036] 1) Experimental materials

[0037] 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), RPMI1640 medium (Gibcol BRL) , RNase A, fetal bovine serum, dimethyl sulfoxide (DMSO), trypsin (Shanghai Bioengineering Co., Ltd.).

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Abstract

The invention discloses a category of cycloastragenol derivatives or pharmaceutically acceptable salt thereof and application thereof to preparation of an anti-hepatic-fibrosis medicament. According to the invention, a microbial conversion technology is utilized to successfully carry out structural modification on cycloastragenol, a plurality of novel compounds are obtained, and in-vitro anti-hepatic-fibrosis cell tests prove that the compounds have good anti-hepatic-fibrosis activities, can be used as active ingredients of the anti-hepatic-fibrosis medicament, and have wide application.

Description

technical field [0001] The invention relates to the field of medicine, in particular to the application of cycloastragenol derivatives in the preparation of drugs for treating liver diseases, and more specifically to the application of cycloastragenol derivatives in the preparation of drugs for preventing and treating liver fibrosis. Background technique [0002] Liver fibrosis refers to the pathological process of proliferation of fibrous connective tissue in the liver when liver cells undergo necrosis and inflammatory stimulation. After various pathogenic factors lead 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 the activity of collagenase also decreases, making the liver The imbalance between the production and degradation of extracellular matrix eventually leads to the excessive deposition of liver collagen a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/56A61K31/58C07J63/00C07J71/00A61P1/16A61P35/00C12P33/20C12R1/785
CPCA61K31/56A61K31/58A61P1/16A61P35/00C07J63/004C07J71/0005C12P33/20
Inventor 宋妍陈广通林海君姜宝成陈晨李建林
Owner 义乌国信白蚁防治有限公司
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