FACTORS AFFECTING THE INTRACELLULAR ACCUMULATION AND ACTIVITY OF AZITHROMYCIN
FACTORS AFFECTING THE INTRACELLULAR ACCUMULATION AND ACTIVITY OF AZITHROMYCIN
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DOI：
10.1093/jac/35.1.85
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发表时间：
1995-01-01
影响因子：
5.2
通讯作者：
PEREA, EJ
中科院分区：
文献类型：
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作者：
PASCUAL, A;CONEJO, MC;PEREA, EJ
阿奇霉素是一种新的大环内酯类抗生素，在人体巨噬细胞中蓄积浓度较高。人多形核白细胞（PMN）中阿奇霉素浓度（固定细胞外浓度1 mg/L）的细胞外比（C/E）受环境温度小幅升高的显著影响（37 ℃和40 ℃时C/E分别为20.3 +/- 2和59.4 +/- 6）。不同浓度的人血清对PMN相关阿奇霉素无影响。当细胞被PMA激活或被酵母多糖调理时，阿奇霉素在细胞内的积累略有下降（C/E约为5）。然而，调理的金黄色葡萄球菌或流感嗜血杆菌的吞噬作用略微增加了阿奇霉素的细胞内浓度。不同浓度阿奇霉素对中性粒细胞产生过氧化氢和超氧阴离子自由基无影响。H.当阿奇霉素浓度高于0.125 mg/L时，人PMN中的流感病毒被消除。然而，在相同的实验条件下，阿奇霉素对S.金黄色
Azithromycin is a new macrolide which accumulates in high concentrations in human phagocytes. The cellular to extracellular ratio (C/E) of azithromycin concentrations (fixed extracellular concentration 1 mg/L) in human polymorphonuclear leucocytes (PMN) were significantly affected by small increases in the environmental temperature (C/E 20.3 +/- 2 and 59.4 +/- 6 at 37 degrees C and 40 degrees C, respectively). PMN-associated azithromycin was not affected by the presence of different concentrations of human serum. The intracellular accumulation of azithromycin decreased slightly (C/E approximately 5) when cells were activated with PMA or opsonized with zymosan. The phagocytosis of opsonized Staphylococcus aureus or Haemophilus influenzae, however, slightly increased the intracellular concentrations of azithromycin. At different extracellular concentrations, azithromycin did not affect the production of hydrogen peroxide and superoxide radicals by PMN. The intracellular survival of H. influenzae in human PMN was abolished in the presence of concentrations higher than 0.125 mg/L of azithromycin. Under the same experimental conditions, however, azithromycin did not show any intracellular activity against S. aureus