Potent growth inhibitory activity of platencin towards multi-drug-resistant and extensively drug-resistant Mycobacterium tuberculosis
Potent growth inhibitory activity of platencin towards multi-drug-resistant and extensively drug-resistant Mycobacterium tuberculosis
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.
720-723
Moustafa, Gamal A. I.
1a452cdc-4856-4243-9864-b391fb115f07
Nojima, Shoji
adfd7059-2c61-4364-b8ef-8ec62829da36
Yamano, Yoshi
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Aono, Akio
9f4da452-59b0-4c5a-9cf4-3b32d1c9107d
Arai, Masayoshi
4990e715-8a30-4f56-a849-f83995a8ebb1
Mitarai, Satoshi
8885e285-0439-496e-8102-1c60cdec4dab
Yoshimitsu, Takehiko
e230a482-aa2a-4285-a4a6-f9752fe6ee34
2013
Moustafa, Gamal A. I.
1a452cdc-4856-4243-9864-b391fb115f07
Nojima, Shoji
adfd7059-2c61-4364-b8ef-8ec62829da36
Yamano, Yoshi
57775773-9dcc-4d87-8734-46b45f2c56c3
Aono, Akio
9f4da452-59b0-4c5a-9cf4-3b32d1c9107d
Arai, Masayoshi
4990e715-8a30-4f56-a849-f83995a8ebb1
Mitarai, Satoshi
8885e285-0439-496e-8102-1c60cdec4dab
Yoshimitsu, Takehiko
e230a482-aa2a-4285-a4a6-f9752fe6ee34
Moustafa, Gamal A. I., Nojima, Shoji, Yamano, Yoshi, Aono, Akio, Arai, Masayoshi, Mitarai, Satoshi and Yoshimitsu, Takehiko
(2013)
Potent growth inhibitory activity of platencin towards multi-drug-resistant and extensively drug-resistant Mycobacterium tuberculosis.
MedChemComm, 4, .
(doi:10.1039/C3MD00016H).
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.
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Accepted/In Press date: 31 January 2013
e-pub ahead of print date: 1 March 2013
Published date: 2013
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Local EPrints ID: 427585
URI: http://eprints.soton.ac.uk/id/eprint/427585
ISSN: 2040-2503
PURE UUID: e57b8f86-50b5-43a9-ba84-530be27277bd
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Date deposited: 23 Jan 2019 17:30
Last modified: 16 Mar 2024 04:40
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Author:
Shoji Nojima
Author:
Yoshi Yamano
Author:
Akio Aono
Author:
Masayoshi Arai
Author:
Satoshi Mitarai
Author:
Takehiko Yoshimitsu
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