Potent growth inhibitory activity of (+/-)-platencin towards multi-drug-resistant and extensively drug-resistant Mycobacterium tuberculosis

作者：Moustafa Gamal A I; Nojima Shoji; Yamano Yoshi; Aono Akio; Arai Masayoshi; Mitarai Satoshi; Tanaka Tetsuaki; Yoshimitsu Takehiko^*

来源：Medchemcomm, 2013, 4(4): 720-723.

DOI：10.1039/c3md00016h

The potent antimycobacterial activity of (+/-)-platencin is reported. Complete inhibition of Mycobacterium smegmatis growth was observed at MICs of 0.5 mu g mL(-1) and 0.3 mu g mL(-1) under aerobic and hypoxic conditions, respectively. Notably, the compound exhibited potent bacteriostatic activities towards Mycobacterium tuberculosis H37Rv (MIC = 2 mu g mL(-1)), multi-drug-resistant M. tuberculosis (MIC = 1 mu g mL(-1)), and extensively drug-resistant M. tuberculosis (MIC = 1 mu g mL(-1)). An overexpression study of the transformants of M. smegmatis revealed that platencin selectively targeted Mt-KasB and modestly inhibited Mt-KasA and Mt-FabH.

• 出版日期2013-4