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dc.contributor.authorSiriporn Kongsoien_US
dc.contributor.authorKazumasa Yokoyamaen_US
dc.contributor.authorApinun Supraserten_US
dc.contributor.authorFuangfa Utrarachkijen_US
dc.contributor.authorChie Nakajimaen_US
dc.contributor.authorOrasa Suthienkulen_US
dc.contributor.authorYasuhiko Suzukien_US
dc.contributor.otherHokkaido Universityen_US
dc.contributor.otherKissei Pharmaceutical Co., Ltd.en_US
dc.contributor.otherKasetsart Universityen_US
dc.contributor.otherMahidol Universityen_US
dc.identifier.citationDrug Testing and Analysis. Vol.7, No.8 (2015), 714-720en_US
dc.description.abstract© 2014 John Wiley & Sons, Ltd. Quinolones exhibit good antibacterial activity against Salmonella spp. isolates and are often the choice of treatment for life-threatening salmonellosis due to multi-drug resistant strains. To assess the properties of quinolones, we performed an in vitro assay to study the antibacterial activities of quinolones against recombinant DNA gyrase. We expressed the S. Typhimurium DNA gyrase A (GyrA) and B (GyrB) subunits in Escherichia coli. GyrA and GyrB were obtained at high purity (>95%) by nickel-nitrilotriacetic acid agarose resin column chromatography as His-tagged 97-kDa and 89-kDa proteins, respectively. Both subunits were shown to reconstitute an ATP-dependent DNA supercoiling activity. Drug concentrations that suppressed DNA supercoiling by 50% (IC<inf>50</inf>s) or generated DNA cleavage by 25% (CC<inf>25</inf>s) demonstrated that quinolones highly active against S. Typhimurium DNA gyrase share a fluorine atom at C-6. The relationships between the minimum inhibitory concentrations (MICs), IC<inf>50</inf>s and CC<inf>25</inf>s were assessed by estimating a linear regression between two components. MICs measured against S. Typhimurium NBRC 13245 correlated better with IC<inf>50</inf>s (R=0.9988) than CC<inf>25</inf>s (R=0.9685). These findings suggest that the DNA supercoiling inhibition assay may be a useful screening test to identify quinolones with promising activity against S. Typhimurium. The quinolone structure-activity relationship demonstrated here shows that C-8, the C-7 ring, the C-6 fluorine, and N-1 cyclopropyl substituents are desirable structural features in targeting S. Typhimurium gyrase.en_US
dc.rightsMahidol Universityen_US
dc.subjectEnvironmental Scienceen_US
dc.titleCharacterization of Salmonella Typhimurium DNA gyrase as a target of quinolonesen_US
Appears in Collections:Scopus 2011-2015

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