Pascual A, García I, Conejo C, Perea E J
Department of Microbiology, School of Medicine, Seville, Spain.
Antimicrob Agents Chemother. 1993 Feb;37(2):187-90. doi: 10.1128/AAC.37.2.187.
The penetration of fluconazole into human polymorphonuclear leukocytes (PMNs) and tissue culture epithelial cells (McCoy) was evaluated. At different extracellular concentrations (0.5 to 10 mg/liter), fluconazole reached cell-associated concentrations greater than the extracellular ones in either human PMNs (intracellular concentration to extracellular concentration ratio, > or = 2.2) or McCoy cells (intracellular concentration to extracellular concentration ratio, > or = 1.3). The uptake of fluconazole by PMNs was rapid and reversible but was not energy dependent. The intracellular penetration of fluconazole was not affected by environmental pH or temperature. Ingestion of opsonized zymosan and opsonized Candida albicans did not significantly increase the amount of PMN-associated fluconazole. At therapeutic extracellular concentrations, the intracellular activity of fluconazole against C. albicans in PMNs was significantly lower than that of amphotericin B. It was concluded that fluconazole reaches high intracellular concentrations within PMNs but shows moderate activity against intracellular C. albicans in vitro.
对氟康唑在人多形核白细胞（PMN）和组织培养上皮细胞（McCoy细胞）中的渗透情况进行了评估。在不同的细胞外浓度（0.5至10毫克/升）下，氟康唑在人PMN（细胞内浓度与细胞外浓度之比，≥2.2）或McCoy细胞（细胞内浓度与细胞外浓度之比，≥1.3）中达到的细胞相关浓度均高于细胞外浓度。PMN对氟康唑的摄取迅速且可逆，但不依赖能量。氟康唑的细胞内渗透不受环境pH值或温度的影响。吞噬调理后的酵母聚糖和调理后的白色念珠菌并未显著增加与PMN相关的氟康唑量。在治疗性细胞外浓度下，氟康唑在PMN中对白色念珠菌的细胞内活性显著低于两性霉素B。得出的结论是，氟康唑在PMN内可达到高细胞内浓度，但在体外对细胞内白色念珠菌的活性中等。
