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Application of epalrestat or pharmaceutically acceptable salt thereof in preparation of medicine for preventing and/or treating bacterial infection diseases

A technology for epalrestat and bacterial infection, applied in the field of biomedicine, which can solve the problems of few types of metallo-β-lactamase inhibitors, few optional drugs for infection treatment, and low safety, so as to overcome bacterial resistance , Improve anti-infection effect, increase sensitivity effect

Pending Publication Date: 2022-03-04
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

[0004] The technical problem to be solved by the present invention is to overcome the deficiencies of the existing metallo-β-lactamase inhibitors with few types, clinical bacterial drug resistance, less optional drugs for infection treatment and low safety, and provide a kind of epalrestat Application of or a pharmaceutically acceptable salt thereof in the preparation of a medicament for preventing and / or treating bacterial infection

Method used

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  • Application of epalrestat or pharmaceutically acceptable salt thereof in preparation of medicine for preventing and/or treating bacterial infection diseases
  • Application of epalrestat or pharmaceutically acceptable salt thereof in preparation of medicine for preventing and/or treating bacterial infection diseases
  • Application of epalrestat or pharmaceutically acceptable salt thereof in preparation of medicine for preventing and/or treating bacterial infection diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Example 1 Detection of epalrestat on the inhibitory activity of IMP-7 metallo-β-lactamases

[0031] test group:

[0032] S1. Firstly mix metallo-β-lactamases (IMP-7, VIM-2, NDM-1 with final concentrations of 2nM, 4nM, 10nM) and different concentrations of epalrestat in buffer in a 96-well plate , incubate at 25°C for 30 minutes to fully combine the inhibitor with the enzyme;

[0033] S2. Add meropenem dissolved in the buffer solution (the final test concentration of IMP-7 and VIM-2 is 50 μM, and the final test concentration of NDM-1 is 100 μM) into a 96-well plate, and measure the change of the absorbance of the system immediately after mixing evenly. Record data.

[0034] Since the absorbance of the substrate meropenem decreases after being hydrolyzed by the enzyme, the degree of hydrolysis of the substrate can be characterized by measuring the change of the absorbance of meropenem. Calculate the residual activity of the enzyme after different concentrations of epal...

Embodiment 2

[0038] Example 2 In vitro antibacterial detection of metallo-β-lactamase inhibitors combined with meropenem

[0039] S1. Inoculum Preparation

[0040] Pick colonies from the fresh culture (Escherichia coli BL21 (DE3) expressing metalloβ-lactamases) cultured on the plate for 18-24 hours, inoculate them into LB liquid medium of 3 mL of kanamycin, and culture After 4 to 6 hours, adjust the colony concentration to 0.5 McFarland turbidimetric standard bacterial suspension, and dilute the above bacterial suspension 1:100 with LB broth before use. During the dilution process, 20mM isopropyl-β-D-thiogalactopyranoside (IPTG) was added at a ratio of 1:20, so that the diluted bacterial solution contained 1mM IPTG.

[0041] S2. Preparation of epalrestat solution and bacterial inoculation

[0042] ① Dilution of meropenem: Prepare 512 μg / mL meropenem solution as the working solution, add 100 μL of the working solution to the first column of the 96-well plate (wells A1-H1), add 50 μL of me...

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PUM

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Abstract

The invention belongs to the technical field of biological medicines, and particularly relates to application of epalrestat or pharmaceutically acceptable salts thereof in preparation of medicines for preventing and / or treating bacterial infection diseases. The epalrestat or the pharmaceutically acceptable salt thereof can inhibit hydrolysis of metal beta-lactamase to beta-lactam antibiotics, so that the sensitivity of drug-resistant microorganisms to the beta-lactam antibiotics is recovered, and the epalrestat or the pharmaceutically acceptable salt thereof has a remarkable effect of assisting in resisting bacterial infection.

Description

technical field [0001] The invention belongs to the technical field of biomedicine. More specifically, it relates to the application of epalrestat or a pharmaceutically acceptable salt thereof in the preparation of medicaments for preventing and / or treating bacterial infection diseases. Background technique [0002] β-lactam antibiotics have been widely used in the clinical treatment of bacterial infections since their invention, but bacteria quickly developed resistance to them, mainly because the bacteria themselves can produce β-lactamase to make β-lactam antibiotics Enzymatic hydrolysis fails. Metallo β-lactamases are a kind of β-lactamases. Common subfamilies include IMP, VIM and NDM. They have stable and efficient carbapenem hydrolysis activity and can catalyze the hydrolysis of monocyclic β-lactamases. All β-lactam antibiotics except lactam drugs, common clinical Gram-negative bacteria such as Klebsiella pneumoniae and E. difficulty. [0003] In order to solve the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/426A61K45/06A61P31/04
CPCA61K31/426A61K45/06A61P31/04Y02A50/30
Inventor 姜志辉杨琰袁进张冰石磊杨晨邹江冰吴琼陈丽丹张海燕
Owner GENERAL HOSPITAL OF SOUTHERN THEATRE COMMAND OF PLA
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