Novel application of betulin derivatives in preparation of drugs for repairing nerve injury

A nerve injury and new application technology, applied in the field of medicine, can solve the problems of incomplete chemical and pharmacological research on betulin derivatives, lack of active groups in the mother nucleus, and few reaction sites, so as to achieve good nerve cell damage repair and protection Activity, enhance the effect of learning and memory ability

Active Publication Date: 2020-08-07
NANTONG UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, pentacyclic triterpenoids have a special structure, the parent nucleus lacks active groups, and there are 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 betulin derivatives with modified core structure are not yet comprehensive, and no literature has reported their neuroprotective effects.

Method used

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  • Novel application of betulin derivatives in preparation of drugs for repairing nerve injury
  • Novel application of betulin derivatives in preparation of drugs for repairing nerve injury
  • Novel application of betulin derivatives in preparation of drugs for repairing nerve injury

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Example 1 Compound I-X has repairing and protective activity on nerve cells damaged by hydrogen peroxide

[0022] (1) Experimental materials

[0023] 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).

[0024] (2) Experimental method

[0025] 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 temper...

Embodiment 2

[0031] Example 2 Effect of compound VI and compound X of the present invention on learning and memory ability of aging mouse model

[0032] (1) Establishment of aging mouse model

[0033] Forty male ICR mice of SPF grade, weighing 22-26 g, were randomly divided into 4 groups, namely control group, model group, compound VI group and compound X group. Except for the control group given normal saline, the mice in the other groups were intraperitoneally injected with D-galactose at a dose of 250 mg / kg, once a day, and the drug group was given 10 mg / kg of the compound by intragastric administration, and the control group and the model group were given intragastric administration, etc. Volumetric saline was administered once daily for 6 weeks. Mice were used for later experiments after showing obvious aging characteristics.

[0034] (2) Experimental method

[0035] The water maze laboratory is an experiment in which experimental animals are forced to swim to find a platform hidde...

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Abstract

The invention provides a novel application of betulin derivatives shown in structural formulas I, II, III, IV, V, VI, VII, VIII, IX and X or pharmaceutically acceptable salts and pharmaceutical compositions of the betulin derivatives in preparation of medicines for repairing nerve injury. The compound can be further used for preparing medicines for treating neurodegenerative diseases, traumatic brain injury and stroke. According to the invention, the medicinal field of the betulin derivative modified by the mother nucleus structure is expanded, and a new choice is provided for developing neuroprotective drugs.

Description

technical field [0001] The invention relates to the field of medicine, in particular to the new application of betulin derivatives in the preparation of medicines for repairing nerve damage. Background technique [0002] The incidence of nervous system diseases such as neurodegenerative diseases, traumatic brain injury and stroke has been increasing year by year, which has brought heavy burdens to society and families. 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. Studying the pathogenesis of these common neurological diseases and finding active and effective treatments 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 caus...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/56A61P25/00A61P25/14A61P25/16A61P25/28
CPCA61K31/56A61P25/00A61P25/14A61P25/16A61P25/28
Inventor 陈广通储呈娇宋开南宋妍李建林
Owner NANTONG UNIVERSITY
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