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Application of sulfydryl-containing compound as and/or in preparation of beta-lactamase inhibitor

A sulfhydryl compound and lactamase technology, applied in the field of medicine, can solve problems such as increased drug resistance, and achieve the effects of reversing drug resistance, improving sensitivity, and good synergistic effect

Active Publication Date: 2021-09-24
GENERAL HOSPITAL OF SOUTHERN THEATRE COMMAND OF PLA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] β-lactam antibiotics are the most important and commonly used antibiotics for the treatment of Gram-negative bacterial infections, but the increasing resistance of bacteria to them in recent years has raised human concerns

Method used

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  • Application of sulfydryl-containing compound as and/or in preparation of beta-lactamase inhibitor
  • Application of sulfydryl-containing compound as and/or in preparation of beta-lactamase inhibitor
  • Application of sulfydryl-containing compound as and/or in preparation of beta-lactamase inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0067] Example 1 Determination of thiol-containing compound to β-lactamase inhibitory activity

[0068] After the substrate is hydrolyzed by the enzyme, the absorbance value will decrease. Therefore, the degree of substrate hydrolysis can be characterized by the change of absorbance, so as to judge the activity of the enzyme. Meropenem (50 μM) was used as the reporter substrate, and the absorbance change of the substrate after being hydrolyzed by metallo-β-lactamase was measured at a wavelength of 300 nm. Metallo-β-lactamases include NDM-1, VIM-2 and IMP-7 at final concentrations of 2nM, 4nM and 5nM, respectively, in a buffer of 50mM HEPES (4-hydroxyethylpiperazineethanesulfonic acid), and the addition of ZnSO 4 (final concentration is 0.1mM), Triton X-100 (final concentration is 0.01% (v / v)), bovine serum albumin (BSA, final concentration is 0.1μg / mL), pH=7.2, reaction temperature is 25°C, the specific experimental method is as follows:

[0069] 1. Determination of the inhi...

Embodiment 2

[0084] Example 2 Evaluation of the combined use of sulfhydryl-containing compounds and meropenem to inhibit β-lactamase-producing drug-resistant bacteria

[0085] The minimum inhibitory concentration (MIC) of sulfhydryl-containing compounds combined with meropenem against β-lactamase-producing resistant strains was determined by micro-broth dilution method. E.coli BL21(DE3) / pMAL-c5x-IMP-7 used in the experiment was purchased from Shanghai Sangon Biotechnology Co., Ltd., E.coli BL21(DE3) / pET24a-VIM-2 and E.coli BL21(DE3) / pET26b-NDM-1 was a gift from Professor Yang Kewu of Northwestern University, and has been in the literature: Zhang Yuejuan, Antibiotic resistance target protein metallo-β-lactamase and its characterization and inhibition of drug-resistant bacteria [D], Northwestern University, Published in 2019; also includes the clinical isolate E.coli BAA-2452 (bla NDM-1 ) and E.coli BAA-2340 (bla KPC-2 ).

[0086] FICI is used to judge the interaction of two drugs when u...

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Abstract

The invention belongs to the field of medicines, and discloses application of a sulfydryl-containing compound as and / or in preparation of a beta-lactamase inhibitor. The invention discloses that the sulfhydryl-containing compound (2-pyrazinyl ethanethiol, 2-methyl-3-tetrahydrofuranethiol, 3-sulfanyl-1-hexanol and 1, 4-butanediol bis (mercaptoacetate)) or the derivative thereof has a good inhibition effect on beta-lactamase (metal beta-lactamase and / or serine beta-lactamase) for the first time, and can protect antibiotics from bacterial degradation, improve bacterial sensitivity to the antibiotics and reverse bacterial resistance to the antibiotics; and meanwhile, the sulfhydryl-containing compound (2-pyrazinyl ethanethiol, 2-methyl-3-tetrahydrofuranethiol and 3-sulfanyl-1-hexanol) and / or the derivative thereof have a good synergistic effect when being combined with antibiotics, and can be used as a composite medicine for inhibiting bacteria.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to the application of thiol-containing compounds as and / or preparing beta-lactamase inhibitors. Background technique [0002] β-lactam antibiotics are the most important and commonly used antibiotics for the treatment of Gram-negative bacterial infections, but the increasing resistance of bacteria to them has caused human concerns in recent years. As one of the β-lactam antibiotics, carbapenem is considered to be the last line of defense against bacterial infections. With the emergence of carbapenemase, human beings gradually lose this most important bargaining chip. [0003] The most important reason for bacterial resistance to β-lactam antibiotics is the production of β-lactamase, which can make antibiotics lose their antibacterial activity by hydrolyzing the lactam ring of β-lactam antibiotics. According to DNA sequence similarity, β-lactamases can be divided into four classe...

Claims

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Application Information

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IPC IPC(8): A61K31/4965A61K31/341A61K31/095A61K31/22A61K45/06A61P31/04
CPCA61K31/4965A61K31/341A61K31/095A61K31/22A61K45/06A61P31/04A61K2300/00Y02A50/30
Inventor 石磊何羡霞张冰姜志辉杨琰袁进蔡敏捷蔡学究李小荣廖扬许文平黄雪峰陈龙浩
Owner GENERAL HOSPITAL OF SOUTHERN THEATRE COMMAND OF PLA
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