Research progress on efflux pump inhibitors of Mycobacterium tuberculosis in recent years
10.16438/j.0513-4870.2023-0373
- VernacularTitle:近年来结核分枝杆菌外排泵抑制剂研究进展
- Author:
Cheng-hong ZHENG
;
Ming-hua WANG
;
Ju-xian WANG
- Publication Type:Research Article
- Keywords:
bacterial resistance;
italic>Mycobacterium tuberculosis;
efflux pump;
efflux pump inhibitor;
antibacterial activity;
structure-activity relationship
- From:
Acta Pharmaceutica Sinica
2023;58(10):2995-3003
- CountryChina
- Language:Chinese
-
Abstract:
Currently, the resistance of first-line anti-tuberculosis drugs has made the prevention and treatment of tuberculosis increasingly difficult, posing a serious threat to global public health. Several studies have shown that efflux pumps are one of the important causes for bacteria to develop multi-drug resistance and extremely-drug resistance, and efflux pump inhibitors can inhibit the efflux of antibacterial drugs, thereby reducing bacterial drug resistance. Numerous natural products and synthetic compounds have been reported to possess efflux pump inhibitory activity, but they have not been applied in clinical settings because of their toxicity, pharmacokinetic properties, etc. Therefore, we summarized the efflux pump inhibitory activity, antimicrobial activity, and structure-activity relationships of reported efflux pump inhibitors against Mycobacterium tuberculosis in recent years, providing references for the development of new efflux pump inhibitors with better activity and lower toxicity.