Ziegler K, Frimmer M
Biochim Biophys Acta. 1984 Oct 12;805(2):174-80. doi: 10.1016/0167-4889(84)90165-4.
Cyclosporin A at concentrations of more than 10 nM protects isolated hepatocytes against the action of phalloidin. Cyclosporin A at 100 nM inhibits the uptake of demethyl[3H]phalloin by 50%, and at 5 microM also that of [14C]cholate. This inhibition is independent of the preincubation period and is not reversed by washing the cells. With a 30-60-fold excess of cyclosporin A, affinity labeling of plasma membrane proteins using 12 microM [3H]isothiocyanatobenzamido cholate was reduced to 40-60% of the control. These findings indicate that transport inhibition by cyclosporin A in liver cells cannot be explained by simple competition on the level of the membrane protein(s) involved.
浓度超过10 nM的环孢素A可保护分离的肝细胞免受鬼笔环肽的作用。100 nM的环孢素A可抑制去甲基[3H]鬼笔环肽摄取50%,5 μM时也可抑制[14C]胆酸盐摄取。这种抑制作用与预温育时间无关,且通过洗涤细胞不能逆转。当环孢素A过量30 - 60倍时,使用12 μM [3H]异硫氰酸苯甲酰胺胆酸盐对质膜蛋白进行亲和标记降低至对照的40 - 60%。这些发现表明,环孢素A对肝细胞转运的抑制不能用所涉及膜蛋白水平上的简单竞争来解释。