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

Research output: Contribution to journal › Article › peer-review

18 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 language	English
Pages (from-to)	720-723
Number of pages	4
Journal	MedChemComm
Volume	4
Issue number	4
DOIs	https://doi.org/10.1039/c3md00016h
Publication status	Published - Apr 2013
Externally published	Yes

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Pharmacology
Pharmaceutical Science
Drug Discovery
Organic Chemistry

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1039/c3md00016h

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title = "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.",

author = "Moustafa, {Gamal A.I.} and Shoji Nojima and Yoshi Yamano and Akio Aono and Masayoshi Arai and Satoshi Mitarai and Tetsuaki Tanaka and Takehiko Yoshimitsu",

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doi = "10.1039/c3md00016h",

language = "English",

volume = "4",

pages = "720--723",

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T1 - Potent growth inhibitory activity of (±)-platencin towards multi-drug-resistant and extensively drug-resistant Mycobacterium tuberculosis

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

PY - 2013/4

Y1 - 2013/4

N2 - 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.

AB - 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.

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DO - 10.1039/c3md00016h

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

Abstract

ASJC Scopus subject areas

UN SDGs

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