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Application of osthole in the preparation of mcr-1 enzyme inhibitor

A technology of MCR-1 and osthole, which can be used in the fields of resisting vector-borne diseases, antibacterial drugs, active ingredients of heterocyclic compounds, etc., and can solve problems such as unseen osthole

Active Publication Date: 2020-10-09
JILIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But up to now, there is no relevant report about osthole in the preparation of MCR-1 inhibitors at home and abroad

Method used

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  • Application of osthole in the preparation of mcr-1 enzyme inhibitor
  • Application of osthole in the preparation of mcr-1 enzyme inhibitor
  • Application of osthole in the preparation of mcr-1 enzyme inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0013] Osthole as an MCR-1 enzyme inhibitor is used in any pharmaceutically acceptable carrier.

Embodiment 2

[0015] The osthole is used as an MCR-1 enzyme inhibitor to prepare medicines for treating infectious diseases.

Embodiment 3

[0017] As an MCR-1 enzyme inhibitor, osthole is used to treat infectious diseases caused by bacteria, especially infections caused by MCR-1-positive enterobacteriaceae.

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Abstract

The invention relates to an application of osthole in preparation of an MCR-1 enzyme inhibitor. A chessboard method and a time-kill curve method prove that the osthole can inhibit activity of MCR-1 enzyme and recover antibacterial activity of polymyxin B for MCR-1 positive enteric bacilli (mainly comprising Escherichia coli and klebsiella pneumoniae). Further, an established mouse thigh muscle infection model proves that the osthole can obviously reduce colony planting of the MCR-1 positive enteric bacilli in combination with the polymyxin B, and meanwhile, toxicity tests prove that the drug concentration of the osthole is non-toxic to mice in the therapeutic dose. Therefore, as the MCR-1 inhibitor, the osthole as the MCR-1 enzyme inhibitor can be combined with antibiotics to increase selectivity to drugs for super drug-resistant bacteria and has great significance in developing new drugs for resisting MCR-1 positive enteric bacilli infection.

Description

technical field [0001] The invention discloses a new application of osthole, further relates to the medical application of osthole in the preparation of MCR-1 enzyme inhibitors, and belongs to the technical field of medical pharmacy. Background technique [0002] The problem of bacterial drug resistance has become a hot spot in the world. In recent years, the infection caused by carbapenemase-producing Gram-negative enterobacteriaceae has become more serious. Drug-resistant bacterial infection has caused carbapenems Antibiotic failure and high mortality rates place greater pressure on treating nosocomial infections, especially ICU infections. This has forced people to use polymyxin, an ancient antibiotic, to control carbapenem-resistant Enterobacteriaceae. However, with the discovery of MCR-1, the "last line" of antibiotic treatment has been broken, and enterobacteriaceae resistant to colistin and carbapenem antibiotics will face no cure. There is no report of an effective...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/37A61P31/04
CPCA61K31/37A61P31/04Y02A50/30
Inventor 邓旭明周永林王建锋
Owner JILIN UNIV
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