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KMID : 0369820090390060431
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Jorunal of Korean Pharmaceutical Sciences
2009 Volume.39 No. 6 p.431 ~ p.435
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시프로플록사신 내성 황색 포도상 구균에서 MIC의 하향 분포로 입증된 DW-224a의 in vitro 항균 활성의 비교 우수성
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Yun Eun-Jeong
Shim Mi-Ja
Choi Eung-Chil
Lee Chun-Yeong
Lee Jong-Seo
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Abstract
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The comparative superior in vitro activity of DW-224a was supported by the downward MIC distribution due to the weakened influence of alterations within target enzymes in ciprofloxacin-resistant Staphylococcus aureus. The MIC50 for DW-224a was 4 μg/mL, similar to that of gemifloxacin, 8-fold less than that of sparfloxacin and 16-over-fold less than that of ciprofloxacin. We constructed combinations of amino acid changes, located at codon 80, 83 or 84 within GrlA and 84, 85 or 88 within GyrA, which were associated with MIC increase. The amino acid changes were less influential to the MIC of DW-224a compared to those of other fluoroquinolones, and it was verified from the requirement of a total of two GrlA- and two GyrA-alterations to reach the MIC of DW-224a over 32 μg/mL.
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KEYWORD
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DW-224a, DNA gyrase, Topoisomerase IV, Quinolone-resistant Staphylococus aureus (QRSA
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