Bryan L E, Van Den Elzen H M
J Antibiot (Tokyo). 1975 Sep;28(9):696-703. doi: 10.7164/antibiotics.28.696.
Gentamicin accumulation with time shows multiphasic kinetics in strains of Escherichia coli and Pseudomonas aeruginosa. All but first phase accumulation may be prevented or reduced by inhibitors of electron transport, by a sulfhydryl poison, by agents which uncouple electron transport and oxidative phosphorylation and by an inhibitor of protein synthesis. The phases of accumulation which are sensitive to these inhibitors are required for loss of cell viability. Gentamicin can be extracted from cells in an unchanged form as judged by paper chromatography and is concentrated 4 to 250 times over extracellular concentrations within the bacterial cell. Gentamicin accumulation has been shown to occur before there is any evidence or release of acid-soluble 3H-adenine from cells. These data demonstrate that productive gentamicin accumulation capable of causing cell death is by active transport.
在大肠杆菌和铜绿假单胞菌菌株中,庆大霉素随时间的积累呈现多相动力学。除第一阶段积累外,电子传递抑制剂、巯基毒物、使电子传递与氧化磷酸化解偶联的试剂以及蛋白质合成抑制剂均可阻止或减少其余阶段的积累。这些抑制剂敏感的积累阶段是细胞活力丧失所必需的。通过纸色谱法判断,庆大霉素可以以未改变的形式从细胞中提取出来,并且在细菌细胞内比细胞外浓度浓缩4至250倍。已表明在细胞有任何酸溶性3H-腺嘌呤释放的证据之前,庆大霉素就已发生积累。这些数据表明,能够导致细胞死亡的有效庆大霉素积累是通过主动转运实现的。