WQ-3810 exerts high inhibitory effect on quinolone-resistant DNA gyrase of Salmonella Typhimurium

Koide, Kentaro; Kongsoi, Siriporn; Nakajima, Chie et al.

Bioscience, Biotechnology, and Biochemistry, 2019, 83(12), 2249-2256

Permalink : https://hdl.handle.net/2115/79881

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アクセス権
open access
URI
https://hdl.handle.net/2115/79881
タイトル
WQ-3810 exerts high inhibitory effect on quinolone-resistant DNA gyrase of Salmonella Typhimurium
著者
Koide, Kentaro ; Kongsoi, Siriporn ; Nakajima, Chie ; Suzuki, Yasuhiko
著者名
Koide, Kentaro
著者名
Kongsoi, Siriporn
著者名
Nakajima, Chie
e-Rad_Researcher
90206540
著者名
Suzuki, Yasuhiko
言語
英語
キーワード
Antimicrobial resistance
fluoroquinolone
Salmonella Typhimurium
IC50
発行日
2019-12-02
出版者
Taylor & Francis
収録物名
Bioscience, Biotechnology, and Biochemistry
巻(号)
83(12)
ページ
2249-2256
抄録
The inhibitory effect of WQ-3810 on DNA gyrase was assayed to evaluate the potential of WQ-3810 as a candidate drug for the treatment of quinolone resistant Salmonella Typhymurium infection. The inhibitory effect of WQ-3810, ciprofloxacin and nalidixic acid was compared by accessing the drug concentration that halves the enzyme activity (IC50) of purified S. Typhimurium wildtype and mutant DNA gyrase with amino acid substitution at position 83 or/and 87 in subunit A (GyrA) causing quinolone resistance. As a result, WQ-3810 reduced the enzyme activity of both wildtype and mutant DNA gyrase at a lower concentration than ciprofloxacin and nalidixic acid. Remarkably, WQ-3810 showed a higher inhibitory effect on DNA gyrase with amino acid substitutions at position 87 than with that at position 83 in GyrA. This study revealed that WQ-3810 could be an effective therapeutic agent, especially against quinolone resistant Salmonella enterica having amino acid substitution at position 87. (Up to 150 words)
資源タイプ
学術雑誌論文
出版タイプ
Accepted Manuscript
権利情報
This is an Accepted Manuscript of an article published by Taylor & Francis in Bioscience, Biotechnology, and Biochemistry on Dec 2nd 2019, available online: http://www.tandfonline.com/10.1080/09168451.2019.1650634 .
PISSN
0916-8451
関連情報 (isVersionOf)
出版社版DOI
https://doi.org/10.1080/09168451.2019.1650634