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

doi:10.1039/c3md00016h

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

研究成果 › 査読

18 被引用数 (Scopus)

抄録

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.

本文言語	English
ページ（範囲）	720-723
ページ数	4
ジャーナル	MedChemComm
巻	4
号	4
DOI	https://doi.org/10.1039/c3md00016h
出版ステータス	Published - 4月 2013
外部発表	はい

ASJC Scopus subject areas

生化学
分子医療
薬理学
薬科学
創薬
有機化学

UN SDG

この成果は、次の持続可能な開発目標に貢献しています

文献へのアクセス

10.1039/c3md00016h

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引用スタイル

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AU - Moustafa, Gamal A.I.

AU - Nojima, Shoji

AU - Yamano, Yoshi

AU - Aono, Akio

AU - Arai, Masayoshi

AU - Mitarai, Satoshi

AU - Tanaka, Tetsuaki

AU - Yoshimitsu, Takehiko

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