Noumi T, Nishida N, Minami S, Watanabe Y, Yasuda T
Research Laboratory, Toyama Chemical Co., Ltd., Japan.
Antimicrob Agents Chemother. 1990 Jun;34(6):949-53. doi: 10.1128/AAC.34.6.949.
The intracellular antimicrobial activity of tosulfoxacin was tested against Salmonella enteritidis C-32 by using human lung fibroid WI-38 cells and was compared with those of ofloxacin and norfloxacin. The intracellular antimicrobial activities of these drugs were evaluated by determining the numbers of viable organisms remaining within cells after treatment with various drug concentrations. At 0.2 and 0.78 microgram/ml, tosufloxacin suppressed intracellular multiplication of S. enteritidis C-32 more effectively than ofloxacin and norfloxacin did. The ability of tosufloxacin to penetrate into WI-38 cells was also determined by the velocity gradient method. The ratio of the intracellular concentration to the extracellular concentration of tosufloxacin was 1.7- and 2.6-fold higher than those of ofloxacin and norfloxacin, respectively. The results indicate that the potent intracellular bactericidal activity of tosufloxacin may be due not only to its high in vitro activity but also to its ability to penetrate into cells at a high level.
采用人肺成纤维细胞WI - 38检测了托氟沙星对肠炎沙门氏菌C - 32的细胞内抗菌活性,并与氧氟沙星和诺氟沙星进行了比较。通过测定不同药物浓度处理后细胞内存活菌数来评估这些药物的细胞内抗菌活性。在0.2和0.78微克/毫升时,托氟沙星比氧氟沙星和诺氟沙星更有效地抑制肠炎沙门氏菌C - 32的细胞内增殖。还通过速度梯度法测定了托氟沙星渗透到WI - 38细胞中的能力。托氟沙星细胞内浓度与细胞外浓度之比分别比氧氟沙星和诺氟沙星高1.7倍和2.6倍。结果表明,托氟沙星强大的细胞内杀菌活性可能不仅归因于其高体外活性,还归因于其高水平渗透到细胞中的能力。