Applications of protopanaxatriol and derivatives thereof in preparation of medicines for treating hepatic disease

A technology of protopanaxatriol and derivatives, which is applied in the field of medicine, can solve the problems of few reaction sites, difficult to prepare derivatives, lack of active groups, etc., and achieves the effect of wide use and good anti-liver fibrosis activity.

Active Publication Date: 2015-02-18
SHENZHEN SUN BIO SCI & TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, protopanaxatriol 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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  • Applications of protopanaxatriol and derivatives thereof in preparation of medicines for treating hepatic disease
  • Applications of protopanaxatriol and derivatives thereof in preparation of medicines for treating hepatic disease
  • Applications of protopanaxatriol and derivatives thereof in preparation of medicines for treating hepatic disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Embodiment 1, preparation of protopanaxatriol derivatives of the present invention

[0022] References Yin Tian, ​​Hongzhu Guo, Jian Han, Dean Guo. Microbial Transformation of 20(S)-Protopanaxatriol by Mucor spinosus. Journal of Natural Products 2005, 68, 678-680; Jie Zhang, Hongzhu Guo, Yin Tian, ​​Peng Liu, Na Li, Jianping Zhou, Dean Guo. Biotransformation of 20(S)-protopanaxatriol by Mucor spinosus and the cytotoxic structure activity relationships of the transformed products. Phytochemistry 2007, 69, 2523-2530 and Guangtong Chen, Xue Yang, Xuguang Zhai, Min Yang .Microbial transformation of 20(S)-protopanaxatriol by Absidia corymbifera and their cytotoxic activities against two human prostate cancer cell lines.Biotechnology Letters 2013,35,91-95 prepared compounds 2-15, 19 and 20 using microbial transformation methods .

[0023] Protopanaxatriol derivatives of the present invention, compounds 1,21,16,17,18 are prepared as follows:

[0024] The invention adopts a m...

Embodiment 2

[0055] Example 2 Anti-hepatic fibrosis activity of protopanaxatriol (PPT) and protopanaxatriol derivatives (compound 1-21) according to the present invention

[0056] 1) Experimental materials

[0057] 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), RPM I1640 medium (Gibcol BRL ), RNase A, fetal bovine serum, dimethyl sulfoxide (DMSO), trypsin (Shanghai Bioengineering Co., Ltd.).

[0058] Cell line for testing: HSC-T6 cell line, which is SD rat hepatic stellate cells transfected with SV40, was purchased from Cancer Institute, Chinese Academy of Medical Sciences.

[0059] Test samples: protopanaxatriol (PPT) and compound 1-21 synthesized in Example 1, with a purity of over 90%, each compound was dissolved in DMSO and then diluted.

[0060] 2) Experimental method

[0061] The half inhibitory rate IC of each t...

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PUM

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Abstract

The invention discloses applications of protopanaxatriol derivatives or pharmaceutically formable salts thereof and protopanaxatriol or pharmaceutically formable salts of the protopanaxatriol in preparation of medicines for treating a hepatic disease. An in-vitro anti-liver fibrosis cell test proves that these compounds have relatively good anti-liver fibrosis activity, can be used as active components of anti-liver fibrosis medicines, and can be applied widely.

Description

technical field [0001] The present invention relates to the field of medicine, in particular to the application of protopanaxatriol and its derivatives in the preparation of drugs with an anti-hepatic fibrosis effect, and more specifically to the application of protopanaxatriol and its derivatives in the preparation of drugs for the prevention and treatment of liver fibrosis in the application. 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. Decrease, the ratio between the production and degradation of extracellular matrix in the liver is unbalanced, and eventually lead to excessive deposition of liver collagen and liver fibrosis. Liver fibrosis continues to deteriorate and lead to liver ci...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/575A61K31/58A61P1/16A61P35/00
CPCA61K31/575A61K31/58
Inventor 陈广通宋妍李建林缪进黄金华
Owner SHENZHEN SUN BIO SCI & TECH CO LTD
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