Gregus Z, Fischer E, Varga F
Arch Int Pharmacodyn Ther. 1979 Mar;238(1):124-33.
In anaesthetized, bile duct-cannulated rats the hepatic transport of bromsulphthalein (BSP) showed a dose-dependent increase in response to simultaneous administration of taurocholate (TC). The excretion rates of both free (BSP) and conjugated bromsulphthalein (BSP-GSH) were significantly elevated by TC. The simultaneously given TC decreased the hepatic uptake of BSP and BSP-GSH, but did not influence the conjugation of BSP with glutathione (GSH) or the biliary excretion rate of exogenous BSP-GSH. When the liver was depleted of GSH by pretreatment with diethyl-maleate (DEM), TC increased the excretion of free BSP. In DEM-treated rats free BSP markedly depressed the biliary excretion of exogenous BSP-GSH. When TC was given simultaneously with BSP, the inhibitory effect of BSP on the excretion of exogenous BSP-GSH was significantly reduced. TC also diminished the depressing effect of BSP on state III respiration of liver mitochondria in vitro. It is concluded that this effect of TC may play a role also in the increased biliary excretion of intraphepatic conjugated BSP.
在麻醉且胆管插管的大鼠中,同时给予牛磺胆酸盐(TC)时,溴磺酞(BSP)的肝转运呈剂量依赖性增加。TC使游离(BSP)和结合型溴磺酞(BSP - GSH)的排泄率均显著升高。同时给予的TC降低了肝脏对BSP和BSP - GSH的摄取,但不影响BSP与谷胱甘肽(GSH)的结合或外源性BSP - GSH的胆汁排泄率。当用马来酸二乙酯(DEM)预处理使肝脏GSH耗竭时,TC增加了游离BSP的排泄。在DEM处理的大鼠中,游离BSP显著抑制外源性BSP - GSH的胆汁排泄。当TC与BSP同时给予时,BSP对外源性BSP - GSH排泄的抑制作用显著降低。TC还减弱了BSP对体外肝线粒体状态III呼吸的抑制作用。结论是,TC的这种作用可能在肝内结合型BSP胆汁排泄增加中也起作用。