Application of compounds Pyrrocidines in preparation of anti-tuberculosis drug

A compound and tuberculosis technology, applied in the field of biology, can solve the problem of lack of new anti-tuberculosis drug screening and other problems, and achieve the effect of high drug availability, abundant sources and low production cost

Inactive Publication Date: 2016-06-22
SUN YAT SEN UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Existing technology lacks the screening of new anti-tuberculosis drugs

Method used

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  • Application of compounds Pyrrocidines in preparation of anti-tuberculosis drug
  • Application of compounds Pyrrocidines in preparation of anti-tuberculosis drug
  • Application of compounds Pyrrocidines in preparation of anti-tuberculosis drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1 Fusion expression of Mycobacterium tuberculosis tyrosine phosphatase B

[0026] (1) Gene cloning of Mycobacterium tuberculosis tyrosine phosphatase B, proceed as follows:

[0027] According to the DNA sequence that inhibits Mycobacterium tuberculosis tyrosine phosphatase B, design and synthesize a pair of primers, add NdeⅠ, XhoⅠ restriction sites to the upstream and downstream primers, and use the genomic DNA of Mycobacterium tuberculosis H37Ra as Template, the 831bp long DNA fragment of Mycobacterium tuberculosis tyrosine phosphatase B was amplified by PCR with the above primers. Electrophoresis and recovers PCR amplified DNA fragments.

[0028] (2) Construction of a vector expressing Mycobacterium tuberculosis tyrosine phosphatase B:

[0029] The plasmid pET28a(+) was extracted, and the DNA fragments of the plasmid and Mycobacterium tuberculosis tyrosine phosphatase B were digested with NdeI and XhoI, and recovered after electrophoresis. The recovered product was ...

Embodiment 2

[0036] Example 2 Analysis of inhibitory enzyme activity of compound Pyrrocidines on Mycobacterium tuberculosis tyrosine phosphatase B

[0037] The enzyme activity of recombinant Mycobacterium tuberculosis tyrosine phosphatase B was analyzed using disodium p-nitrophenyl phosphate (pNPP) as the substrate. The Mycobacterium tuberculosis tyrosine phosphatase B used was purified in Example 1. The recombinant Mycobacterium tuberculosis tyrosine phosphatase B fusion protein. The 500mMpNPP stock solution stored at -20°C is dissolved on ice, and pNPP and MptpB are diluted appropriately with reaction buffer (50mMTris, 100mMNaCl, pH7.8). In a 96-well plate, add MptpB at a final concentration of 6μg / mL, a concentration gradient of compounds (0μM, 3.9μM, 7.8μM, 15.6μM, 31.25μM, 62.5μM, 125μM, 250μM), 1.5mM pNPP, total reaction The volume is 200 μL. React at 37°C for 5 min, and read the absorbance value of each well at 405 nm by a light absorption microplate reader. According to the absorba...

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Abstract

The invention provides an application of compounds Pyrrocidines in preparation of an anti-tuberculosis drug, namely, an application of the compounds Pyrrocidines, derivatives of the compound Pyrrocidines or pharmaceutically acceptable salts of the compounds Pyrrocidines as tyrosine phosphatase inhibitors or in preparation of the tyrosine phosphatase inhibitors. The compounds 19-O-methyl-pyrrrocidine B and pyrrrocidine B have inhibitory activity on mycobacterium tuberculosis tyrosine phosphatase B, and IC50 of the compounds is 3.9 mu M and 75.5 mu M respectively. The compounds can effectively inhibit dephosphorylation activity of the mycobacterium tuberculosis tyrosine phosphatase B and has the clinical application potential for tuberculosis treatment; besides, the compounds Pyrrocidines are natural-metabolism active micro-molecular products separated from microorganisms and can be produced through chemical synthesis and large-scale fermentation separation, the sources are abundant, the production cost is low, and the possibility of medicine preparation is high.

Description

Technical field [0001] The invention relates to the field of biological technology, and more specifically, to the application of the compound Pyrrocidines in the preparation of anti-tuberculosis drugs. Background technique [0002] Tuberculosis is a chronic infectious disease caused by Mycobacterium tuberculosis and one of the most deadly infectious diseases in the world. According to the World Health Organization's 2014 Global Tuberculosis Control Report, in 2013, 9 million people contracted tuberculosis and 1.5 million died. Although China’s tuberculosis cases and death rates have continued to drop significantly in the past two decades, China is still one of the world’s top ten countries with a high incidence of tuberculosis, and drug-resistant tuberculosis is on the rise. At present, the situation of tuberculosis prevention and treatment is still very serious. [0003] Mycobacterium tuberculosis is an intracellular pathogen. After entering the lungs, the bacteria will be swall...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/407A61P31/06
CPCA61K31/407
Inventor 陆勇军陈冬妮蒋思萍许佳怡刘岚李静陈彬
Owner SUN YAT SEN UNIV
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