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

Gamal A.I. Moustafa, Shoji Nojima, Yoshi Yamano, Akio Aono, Masayoshi Arai, Satoshi Mitarai, Tetsuaki Tanaka, Takehiko Yoshimitsu

Research output: Contribution to journalArticle

13 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)720-723
Number of pages4
JournalMedChemComm
Volume4
Issue number4
DOIs
Publication statusPublished - Apr 2013
Externally publishedYes

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry

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