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

Abstract

The potent antimycobacterial activity of (±)-platencin is reported. Complete inhibition of Mycobacterium smegmatis growth was observed at MICs of 0.5 μg mL⁻¹ and 0.3 μg mL⁻¹ under aerobic and hypoxic conditions, respectively. Notably, the compound exhibited potent bacteriostatic activities towards Mycobacterium tuberculosis H37Rv (MIC = 2 μg mL⁻¹), multi-drug-resistant M. tuberculosis (MIC = 1 μg mL⁻¹), and extensively drug-resistant M. tuberculosis (MIC = 1 μg 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.