Application of Panaxadiol Derivatives in Preparation of Drugs for Preventing or Treating Liver Diseases

A kind of Panaxadiol, Derivative Technology

Active Publication Date: 2017-09-26
苏州康纯医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, panaxadiol 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 Panaxadiol Derivatives in Preparation of Drugs for Preventing or Treating Liver Diseases
  • Application of Panaxadiol Derivatives in Preparation of Drugs for Preventing or Treating Liver Diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Embodiment 1, structural formula is the preparation of the compound of 1-8

[0019] Compounds 1 and 2 were prepared according to the methods disclosed in Phytochemistry Letters 2009, 2, 63-66 and Bioorganic & Medicinal Chemistry 2009, 17(8), 3003-3010.

[0020] The invention adopts a microbial conversion method, takes panaxadiol as a raw material, and undergoes steps such as fermentation, extraction, and separation to prepare the compound of the invention. Microorganisms capable of transformation include: Absidia, Cunninghamella, Mucor, Alternaria, Rhodotorula, Syncephalastrum or Rhizopus (Rhizopus) microorganisms; Among them, strains of Absidia and Mucor have stronger transforming ability. These strains can be purchased from the Chinese Academy of Sciences Microbial Culture Collection Center (CGMCC) or the China Institute of Food Fermentation Industrial Microbiology Collection Center (CICC), and stored on a solid slant medium in a refrigerator at 4 °C. Potato medium ...

Embodiment 2

[0035] Example 2 Anti-hepatic fibrosis activity of compounds 1-8 of the present invention

[0036] 1) Experimental materials

[0037] Instruments and reagents: CO 2Incubator (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 the application of a class of panaxadiol derivatives or pharmaceutically acceptable salts thereof in the preparation of drugs for preventing or treating liver diseases. The present invention utilizes microbial transformation technology to successfully modify the structure of panaxadiol and obtain various novel compounds, which are confirmed by in vitro anti-hepatic fibrosis cell tests, and these compounds have good anti-hepatic fibrosis activity and can be used as anti-hepatic fibrosis. The active ingredient of liver fibrosis medicine has a wide range of uses.

Description

technical field [0001] The invention relates to the field of medicine, in particular to the application of panaxadiol derivatives in the preparation of medicines for preventing or treating liver diseases, and more specifically to the application of panaxadiol derivatives in the preparation of medicines for preventing and treating liver fibrosis. 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 cirrhosis and even liver cancer, so the chain of "hep...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/58A61P1/16A61P35/00A61P29/00C12P33/20C12R1/645C12R1/785C12R1/845
Inventor 陈广通宋妍李建林缪进吴娟娟
Owner 苏州康纯医药科技有限公司
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