红霉素进入艾氏小鼠腹水瘤细胞的动力学
Kinetics of erythromycin uptake into Ehrlich mouse ascites tumor cells.
作者信息
Dette G A, Knothe H
机构信息
Zentrum der Hygiene, Abteilung für Medizinische Mikrobiologie, Johann Wolfgang Goethe-Universität, Frankfurt/Main, Fed. Rep. of Germany.
出版信息
Arzneimittelforschung. 1987 Jul;37(7):799-802.
The uptake was studied with freshly isolated Ehrlich ascites tumor (EMAT) cells and with 14C-labelled erythromycin. Erythromycin was accumulated by EMAT cells. The uptake rates and quotes of erythromycin increased with increasing temperature and with increasing pH value (alkaline pH). The uptake was reduced by SH-group reagents, by inhibitors of electron transport and of oxidative phosphorylation and by ouabain. The uptake was saturable (Km = 6.0 X 10(-4) mol/l). The release of the accumulated erythromycin followed first order kinetics (k = 4.5 X 10(-2) min-1). The uptake and accumulation of erythromycin cannot be explained by non-ionic partition. An active uptake mechanism is suggested.
采用新鲜分离的艾氏腹水瘤（EMAT）细胞和14C标记的红霉素研究摄取情况。EMAT细胞能积累红霉素。红霉素的摄取速率和摄取量随温度升高以及pH值升高（碱性pH）而增加。摄取会被巯基试剂、电子传递和氧化磷酸化抑制剂以及哇巴因降低。摄取具有饱和性（Km = 6.0×10⁻⁴mol/L）。积累的红霉素的释放遵循一级动力学（k = 4.5×10⁻²min⁻¹）。红霉素的摄取和积累不能用非离子分配来解释。提示存在一种主动摄取机制。
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