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Application of betulinic acid derivatives in preparation of medicine for treating cardiovascular diseases

A betulinic acid and cardiovascular technology, applied in the field of medicine, can solve the problems of lack of active groups in the nucleus, few reaction sites, and less research on betulinic acid derivatives, so as to achieve good cardiomyocyte protection activity, Widely Useful Effects

Inactive Publication Date: 2021-11-30
NANTONG UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the special structure of pentacyclic triterpenoids, the mother nucleus lacks active groups and few reaction sites. It is difficult to modify the mother nucleus structure by conventional chemical reaction methods to obtain derivatives with hydroxyl, carbonyl and other modifications on the mother nucleus. , therefore, less research has been done on betulinic acid derivatives with structural modification of the core

Method used

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  • Application of betulinic acid derivatives in preparation of medicine for treating cardiovascular diseases
  • Application of betulinic acid derivatives in preparation of medicine for treating cardiovascular diseases
  • Application of betulinic acid derivatives in preparation of medicine for treating cardiovascular diseases

Examples

Experimental program
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Effect test

Embodiment 1

[0019] Preparation of compounds of formula formula Ⅰ- formula XVI: Example 1

[0020] The present invention is a method using a microbial conversion to betulin acid as raw material, after fermentation, extraction and separation steps, to prepare compounds of the present invention. Rhizopus (Rhizopus) are available commercially from a strain of the genus Culture Collection Center, Chinese Academy (CGMCC), potato selection medium, stored in the solid slant culture on opposite 4 ℃ refrigerator.

[0021] In Rhizopus arrhizus Rhizopus arrhizus CGMCC 3.868 as an example, the preparation of the compounds of the formula formula formula XVI Ⅰ- follows:

[0022] 1) Fermentation, transformation, and extraction

[0023] The Rhizopus arrhizus Rhizopus arrhizus CGMCC 3.868 Access two 250mL flask (with potato 100mL medium), as a seed liquid. After 1 day of shaking on the shaker, 26 ° C was oscillated for 1 day, the growth of the bacteria was in a strong period, and 1 ml of seed fluid was suckled...

Embodiment 2

[0054] Example 2: Compound I-XVI on myocardial cell protection activity damaged by hydroperoxide

[0055] (1) Experimental materials

[0056] CO 2Culture Box (Jouan IGO150); enzyme standard (Bio-Tek Elx800); fluorescence inverted microscope (Olympusix51); MTT cell proliferation and cytotoxic detection kit (Biyun Sky Biotechnology Research Institute), DMEM High Sugar Media (Gibcol BRL ), Fetal bovine serum, dimethyl sulfoxide (DMSO), trypsin (Shanghai Bioengineering Co., Ltd.), 30% hydrogen peroxide (H 2 O 2 (Tianjin Ruijin Characterization Co., Ltd.), H9C2 cells (Institute of Tumor, Chinese Academy of Medical Sciences).

[0057] (2) Experimental method

[0058] Each trial compound is determined by MTT method 2 O 2 Influence of damaged H9C2 cell activity: After digestion with pancreatic enzyme, the cellular density of cell suspension is adjusted to 5 × 10 4 2 μl of each well in 96-well culture plates, placed in 5% CO 2 , 37 ° C constant temperature CO 2 The culture tank was culture...

Embodiment 3

[0066] Example 3 Protective effect of Compound I-XVI on myocardial cytracychemia and reperfusion injury

[0067] 1) Experimental materials

[0068] CO 2 Culture Box (Jouan IGO150); enzyme standard (Bio-Tek Elx800); fluorescence inverted microscope (Olympusix51); MTT cell proliferation and cytotoxic detection kit (Biyun Sky Biotechnology Research Institute), DMEM High Sugar Media (Gibcol BRL ), Fetal bovine serum, dimethyl sulfoxide (DMSO), trypsin (Shanghai Biological Engineering Co., Ltd.), H9C2 Cells (Institute of Tumors, Chinese Academy of Medical Sciences).

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Abstract

The invention belongs to the technical field of medicines, and discloses application of betulinic acid derivatives in preparation of medicine for treating cardiovascular diseases. According to the invention, a microbial conversion technology is utilized to successfully carry out structural modification on betulin acid, and 16 novel betulin acid derivatives with modified parent nucleus structures are obtained. In-vitro myocardial cell injury protection tests and myocardial cell ischemia reperfusion tests prove that the compounds have good myocardial cell protection activity, can be used as active ingredients of drugs for treating myocardial infarction, coronary atherosclerotic heart disease and chronic heart failure, and can be applied to preparation of drugs for treating cardiovascular diseases.

Description

Technical field [0001] The present invention relates to the field of medical technology, in particular to apply a betulin acid derivatives in the manufacture of a medicament in the treatment of cardiovascular diseases. Background technique [0002] With the improvement of living standards and population aging, the incidence of cardiovascular disease has increased year by year, and has become one of the highest human mortality. In the process of developing a variety of cardiomyocytes injury in a variety of cardiovascular diseases such as myocardial infarction, ischemia-reperfusion injury, thereby causing cell apoptosis, causing disorders of cardiovascular function. Myocardial ischemia and oxidative stress are an important factor in cardiovascular disease. [0003] Betulinic acid also known as betulin acid, is a lupane-type pentacyclic triterpenoid compounds, mainly from birch bark, is also present in apple, quisqualate, and Vitex negundo boxwood plants. Modern pharmacological stud...

Claims

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Application Information

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IPC IPC(8): A61K31/56A61K31/704A61P9/00A61P9/04A61P9/10C12P33/20C12P33/00C12P33/06C12P33/08C12R1/845
CPCA61K31/56A61K31/704A61P9/00A61P9/04A61P9/10C12P33/20C12P33/00C12P33/06C12P33/08
Inventor 陈广通吴艳妮朱心娟陆游佳范博义宋妍
Owner NANTONG UNIVERSITY
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