Application of osthole in preparation of MCR-1 enzyme inhibitor

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...

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