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Application of ursolic acid derivatives in the preparation of medicines for treating nervous system diseases

A technology of ursolic acid and derivatives, applied in the field of medicine, can solve the problems of difficulty in obtaining derivatives, lack of active groups in the parent nucleus, incomplete chemical and pharmacological research on ursolic acid derivatives, etc., and achieve good repair of nerve cell damage. and anti-neuroinflammatory activity

Active Publication Date: 2022-02-01
NANTONG UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the special structure of pentacyclic triterpenoids, the parent nucleus lacks active groups and few reaction sites, it is difficult to obtain derivatives with hydroxyl, carbonyl and other modifications on the parent nucleus by conventional chemical reaction methods
Therefore, the chemical and pharmacological studies of ursolic acid derivatives with structural modification of the core are not yet comprehensive

Method used

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  • Application of ursolic acid derivatives in the preparation of medicines for treating nervous system diseases
  • Application of ursolic acid derivatives in the preparation of medicines for treating nervous system diseases
  • Application of ursolic acid derivatives in the preparation of medicines for treating nervous system diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Embodiment 1, structural formula is the preparation of the compound of formula I-formula IV

[0021] The invention adopts a microbial conversion method, uses ursolic 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.

[0022] Taking Circinella muscae CGMCC 3.2695 as an example, the process of preparing the compound whose structural formula is formula I-Formula IV is as follows:

[0023] 1) Fermentation, transformation and extraction

[0024] 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 stage,...

Embodiment 2

[0031] Example 2 Compounds Ⅰ-Ⅳ have repairing and protective activity on nerve cells damaged by hydrogen peroxide

[0032] (1) Experimental materials

[0033] CO 2 Incubator (Jouan IGO150); Microplate reader (Bio-TEK ELx800); Fluorescent inverted microscope (OlympusIX51); MTT cell proliferation and cytotoxicity detection kit (Biotech Institute), DMEM high glucose medium (Gibcol BRL ), fetal bovine serum, dimethyl sulfoxide (DMSO), trypsin (Shanghai Bioengineering Co., Ltd.), 30% hydrogen peroxide (H 2 o 2 ) (Tianjin Ruijinte Chemicals Co., Ltd.), SH-SY5Y cells (Tumor Institute, Chinese Academy of Medical Sciences).

[0034] (2) Experimental method

[0035] The MTT method was used to determine the H of each test compound 2 o 2 Influence of damaged SH-SY5Y cell viability: count the cells after digestion with trypsin, adjust the cell density of the cell suspension to 5×10 4 cells / mL, add 200 μL to each well of a 96-well culture plate, place in 5% CO 2 , 37°C constant temp...

Embodiment 3

[0042] Example 3 Anti-neuroinflammatory activity of compounds Ⅰ-Ⅳ of the present invention

[0043] 1) Experimental materials

[0044]Instruments and reagents: CO2 incubator (Jouan IGO150); microplate reader (Bio-TEK ELx800); fluorescent inverted microscope (Olympus IX51); MTT cell proliferation and cytotoxicity detection kit (Beiyuntian Biotechnology Institute), RPMI 1640 Medium (Gibcol BRL), microglial cells BV-2, RNase A, fetal bovine serum, dimethyl sulfoxide (DMSO), trypsin (Shanghai Bioengineering Co., Ltd.).

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Abstract

The invention belongs to the field of medicine and discloses the application of a class of ursolic acid derivatives in the preparation of medicines for treating nervous system diseases. The present invention utilizes microbial transformation technology to successfully modify the structure of ursolic acid, and obtains 4 novel compounds with structural modification of the mother nucleus, which are confirmed by in vitro nerve cell injury protection tests and neuroglial cell inflammation tests. The compound has better nerve cell protection activity and anti-neurinflammation activity, can be used as an active ingredient of drugs for treating neurodegenerative diseases, traumatic brain injury, and stroke, and has wide applications.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to the application of ursolic acid derivatives in the preparation of medicines for treating nervous system diseases. Background technique [0002] With the intensification of aging, the incidence of neurodegenerative diseases, traumatic brain injury and stroke and other neurological diseases are increasing year by year. Current clinical drugs can only alleviate some symptoms, but cannot effectively prevent the occurrence of the disease, improve the cognitive status of patients and prevent the development of the disease. Finding active and effective treatment methods has become an urgent task in neuroscience and other related disciplines. During the occurrence and development of the above-mentioned diseases, the damage, loss or death of nerve cells in the brain is the most basic pathological change, which often causes severe damage to nerve function and leads to hemiplegia, aphas...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/56A61P25/00A61P25/28A61P25/16A61P25/14A61P21/00A61P9/10C12P33/00C12R1/645
CPCA61K31/56A61P25/00A61P25/28A61P25/16A61P25/14A61P21/00A61P9/10C12P33/00
Inventor 陈广通陆游佳徐天怡储呈娇宋开南宋妍
Owner NANTONG UNIVERSITY
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