Transport of cyclosporin A in kidney epithelial cell line (LLC-PK1).
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.
Takayama
A
A
Department of Pharmacy, Kyoto University Hospital, Faculty of Medicine, Kyoto University, Japan.
Okazaki
Y
Y
Fukuda
K
K
Takano
M
M
Inui
K
K
Hori
R
R
D000818:Animals; D001692:Biological Transport / Q000187:drug effects; D002460:Cell Line; D003524:Cyclosporins / Q000493:pharmacokinetics* / Q000633:toxicity; D007668:Kidney / Q000187:drug effects / Q000378:metabolism*; D013552:Swine; D013696:Temperature; D014700:Verapamil / Q000494:pharmacology
D003524:Cyclosporins; D014700:Verapamil