曲伐沙星在人吞噬细胞和组织培养上皮细胞中的摄取及细胞内活性。
Uptake and intracellular activity of trovafloxacin in human phagocytes and tissue-cultured epithelial cells.
作者信息
Pascual A, García I, Ballesta S, Perea E J
机构信息
Department of Microbiology, School of Medicine, University of Seville, Spain.
出版信息
Antimicrob Agents Chemother. 1997 Feb;41(2):274-7. doi: 10.1128/AAC.41.2.274.
Abstract
The penetration of trovafloxacin into human polymorphonuclear leukocytes (PMNs), human peritoneal macrophages, and tissue-cultured epithelial cells (McCoy cells) was evaluated. The cellular concentration to extracellular concentration (C/E) ratios of trovafloxacin were greater than 9 for extracellular concentrations ranging from 0.5 to 25 micrograms/ml. The uptake of trovafloxacin by PMNs was rapid, reversible, nonsaturable, not energy dependent, and significantly increased at 4 degrees C. Ingestion of opsonized zymosan, but not opsonized Staphylococcus aureus, significantly increased the amount of PMN-associated trovafloxacin. This agent at concentrations of 0.5 and 1 microgram/ml induced a greater reduction in the survival of intracellular S. aureus in PMNs than ciprofloxacin and ofloxacin. It was concluded that trovafloxacin reaches concentrations within phagocytic and nonphagocytic cells several times higher than the extracellular ones, while it remains active in PMNs.
摘要
评估了曲伐沙星在人多形核白细胞（PMN）、人腹膜巨噬细胞和组织培养上皮细胞（ McCoy细胞）中的渗透情况。对于0.5至25微克/毫升的细胞外浓度范围，曲伐沙星的细胞内浓度与细胞外浓度（C/E）之比大于9。PMN对曲伐沙星的摄取迅速、可逆、不饱和、不依赖能量，且在4℃时显著增加。吞噬调理酵母聚糖而非调理金黄色葡萄球菌可显著增加与PMN相关的曲伐沙星量。该药物在0.5和1微克/毫升浓度下比环丙沙星和氧氟沙星能更有效地降低PMN内细胞内金黄色葡萄球菌的存活率。结论是，曲伐沙星在吞噬细胞和非吞噬细胞内达到的浓度比细胞外浓度高几倍，同时在PMN中仍保持活性。
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