Niwa M, Hotta K, Kanamori Y, Matsuno H, Kozawa O, Hirota M, Uematsu T
Department of Pharmacology, Gifu University School of Medicine, Gifu City, Japan.
Eur J Pharmacol. 2001 Sep 28;428(1):121-6. doi: 10.1016/s0014-2999(01)01273-0.
The uptake of the antimicrobial quinolone agent, grepafloxacin, both by human circulating blood neutrophils and by those exudated into tissues, was evaluated in vitro by comparing the intracellular drug concentrations. In circulating blood neutrophils, the uptake of grepafloxacin was rapid and saturable at 37 degrees C. The uptake of grepafloxacin into circulating blood neutrophils was reduced by lowering the environmental temperature or by the presence of metabolic inhibitors, suggesting the involvement of an active transport mechanism. Furthermore, the uptake of grepafloxacin by tissue (salivary) neutrophils was also partially temperature-dependent and was significantly greater than that by circulating blood neutrophils, i.e. exudation of neutrophils into tissue results in a markedly enhanced transport mechanism for grepafloxacin. This phenomenon may be related to the higher defense activity against infection seen in exudated tissue neutrophils.
通过比较细胞内药物浓度，在体外评估了人类循环血液中性粒细胞和渗出到组织中的中性粒细胞对抗菌喹诺酮类药物格帕沙星的摄取情况。在循环血液中性粒细胞中，格帕沙星在37℃时的摄取迅速且具有饱和性。降低环境温度或存在代谢抑制剂会减少格帕沙星进入循环血液中性粒细胞的摄取，这表明存在主动转运机制。此外，组织（唾液）中性粒细胞对格帕沙星的摄取也部分依赖温度，且明显高于循环血液中性粒细胞，即中性粒细胞渗出到组织中会导致格帕沙星的转运机制显著增强。这种现象可能与渗出组织中的中性粒细胞对感染具有更高的防御活性有关。
