Takayama A, Okazaki Y, Fukuda K, Takano M, Inui K, Hori R
Department of Pharmacy, Kyoto University Hospital, Faculty of Medicine, Kyoto University, Japan.
J Pharmacol Exp Ther. 1991 Apr;257(1):200-4.
The characteristics of cyclosporin A transport have been studied in cultured kidney epithelial cell line LLC-PK1. The uptake of cyclosporin A by LLC-PK1 cells was time-dependent and reached a steady state at about 30 min. The initial uptake was saturable and was inhibited by cyclosporin A analogs, cyclosporin C and D and by verapamil, but not by metabolic inhibitors such as 2,4-dinitrophenol and rotenone. Cyclosporin A uptake as well as efflux was strongly dependent on temperature. The Arrhenius plot for cyclosporin A uptake was biphasic, whereas the Arrhenius plot for sulfanilamide uptake, which is transported by a simple diffusion, was linear. These results indicate that a specific mechanism is concerned in the transport of cyclosporin A in LLC-PK1, cells.
已在培养的肾上皮细胞系LLC-PK1中研究了环孢素A的转运特性。LLC-PK1细胞对环孢素A的摄取具有时间依赖性，约30分钟时达到稳态。初始摄取是可饱和的，并且受到环孢素A类似物、环孢素C和D以及维拉帕米的抑制，但不受2,4-二硝基苯酚和鱼藤酮等代谢抑制剂的抑制。环孢素A的摄取和流出都强烈依赖于温度。环孢素A摄取的阿伦尼乌斯曲线是双相的，而通过简单扩散转运的磺胺摄取的阿伦尼乌斯曲线是线性的。这些结果表明，LLC-PK1细胞中环孢素A的转运涉及一种特定机制。
