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Application of bazedoxifene acetate in anti-mycobacterium tuberculosis drugs

A bazedoxifene acetate and anti-tuberculosis technology, applied in the field of bioengineering, can solve the problems of cross-drug resistance, lack of effective diagnostic technology, slow development of anti-tuberculosis drugs, etc., and achieve high safety, good development value, and enhanced cell killing The effect of tuberculosis

Active Publication Date: 2022-02-18
SHENZHEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Due to the lack of effective preventive vaccines and effective diagnostic techniques, overcoming clinical drug resistance is a major topic and research hotspot in the prevention and control of tuberculosis. However, the development of new and effective anti-tuberculosis drugs is slow, and these drugs directly act on tuberculosis itself. There is always a risk of cross-resistance

Method used

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  • Application of bazedoxifene acetate in anti-mycobacterium tuberculosis drugs
  • Application of bazedoxifene acetate in anti-mycobacterium tuberculosis drugs
  • Application of bazedoxifene acetate in anti-mycobacterium tuberculosis drugs

Examples

Experimental program
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Effect test

Embodiment 1

[0022] 1. Differentiation of U937 macrophages (No. BNCC100967): Suspended U937 macrophages were cultured in RPMI-1640 medium containing 10% FBS, and placed at a temperature of 37 ° C, containing 5% CO 2 Cultured in a cell incubator, added PMA with a final concentration of 20ng / ml, cultured overnight, differentiated into macrophages, washed twice with PBS, digested with trypsin, resuspended, added to a 96-well cell culture plate , so that the number of cells per well is 1x104;

[0023] 2. Determination of cell survival rate: After the above-mentioned U937 macrophages were cultured for 24 hours, different concentrations of drugs were added to make the final drug concentrations 100uM, 10uM, and 1uM. The experiment was repeated three times for each concentration, and DMSO was used as a parallel control experiment. In the control group, DMSO with the same volume as the drug was added, and the experiment was repeated three times. After 48 hours, 10ul of WST-1 solution was added to e...

Embodiment 2

[0029] 1. Differentiation of U937 macrophages: Suspended U937 macrophages were cultured in RPMI-1640 medium containing 10% FBS, and placed in a temperature of 37 ° C, containing 5% CO 2 Cultured in a cell incubator, added PMA with a final concentration of 20ng / ml, cultured overnight, differentiated into macrophages, washed twice with PBS, digested with trypsin, resuspended, added to a 96-well cell culture plate , so that the number of cells per well is 1x104;

[0030] 2. Infection of U937 cells with Mycobacterium tuberculosis: After culturing the above-mentioned U937 macrophages, add Mycobacterium tuberculosis to infect U937 cells. After infection, wash the cells twice with PBS, and then add fresh medium;

[0031] 3. Determination of intracellular bactericidal activity: After the above-mentioned U937 macrophages were cultured for 24 hours, bazedoxifene acetate was added to make the final concentration 10uM, and the experiment was repeated three times for each concentration, us...

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Abstract

The invention relates to the application of bazedoxifene acetate in anti-tuberculosis mycobacterium drugs. Bazedoxifene acetate is the third generation selective estrogen receptor modulator; And the present invention research finds that it has the effect of anti-tuberculosis, has good development value; The application in mycobacterium medicine and the obvious anti-tuberculosis mycobacterium effect of bazedoxifene acetate are disclosed for the first time.

Description

technical field [0001] The invention relates to the technical field of bioengineering, in particular to the application of bazedoxifene acetate in anti-tuberculosis mycobacterium drugs. Background technique [0002] Due to the lack of effective preventive vaccines and effective diagnostic techniques, overcoming clinical drug resistance is a major topic and research hotspot in the prevention and control of tuberculosis. However, the development of new and effective anti-tuberculosis drugs is slow, and these drugs directly act on tuberculosis itself. There is always a risk of cross-resistance. [0003] Bazedoxifene acetate is a third-generation selective estrogen receptor modulator (SERM) approved in the European Union and Japan, and in advanced stages of review by the U.S. Food and Drug Administration (FDA). The mechanism of action of bazedoxifene acetate is unique. As a new type of selective estrogen receptor modulator (SERM), it can selectively regulate estrogen receptors,...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/55A61P31/06
CPCA61K31/55A61P31/06
Inventor 蔡毅陈心春欧阳琪
Owner SHENZHEN UNIV
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