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- Title
WQ-3810 exerts high inhibitory effect on quinolone-resistant DNA gyrase of Salmonella Typhimurium.
- Authors
Koide, Kentaro; Kongsoi, Siriporn; Nakajima, Chie; Suzuki, Yasuhiko
- Abstract
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. WQ-3810 shows high inhibitory activity against quinolone resistant DNA gyrase.
- Subjects
DNA topoisomerase II; SALMONELLA typhimurium; SALMONELLA diseases; SALMONELLA enterica; AMINO acids; BETA lactamases
- Publication
Bioscience, Biotechnology & Biochemistry, 2019, Vol 83, Issue 12, p2249
- ISSN
0916-8451
- Publication type
Article
- DOI
10.1080/09168451.2019.1650634