Mahu J L, Duvaldestin P, Dhumeaux D, Berthelot P
Am J Physiol. 1977 May;232(5):E445-50. doi: 10.1152/ajpendo.1977.232.5.E445.
The hepatobiliary transport of three structurally related phthaleins was compared in the rat, and found to differ to a large extent in three experimental conditions: 1) after a 72-h fast; 2) after a 4-day phenobarbital treatment; and 3) during infusion of bile salts: sodium dehydrocholate or taurocholate. In the fasting group, bile flow and bile salt excretion (on a whole liver basis) decreased by 49 and 41%, respectively; bromsulphthalein sodium (BSP) and dibromsulphthalein sodium (DBSP) transport maximum (Tm) were reduced by 59 and 50%; however, rose bengal (RB) Tm remained normal. Phenobarbital pretreatment yielded a 44 and 29% increase in BSP and DBSP Tm, respectively, whereas RB Tm remained unchanged. Dehydrocholate infusion caused a 27 and 49% increase in BSP and DBSP Tm, whereas RB Tm increased by 12%. On the contrary, equimolar taurocholate infusion yielded a more important increase in RB Tm (56%) than in BSP and DBSP (31 and 22% respectively). It is suggested that RB does not share the same liver-to-bile excretory pathway as that of the former molecules. Our results emphasize the difficulties in predicting the biliary excretion of foreign compounds, even when their structure is closely similar.
在大鼠中比较了三种结构相关的酞类化合物的肝胆转运情况，发现在三种实验条件下差异很大：1）禁食72小时后；2）苯巴比妥治疗4天后；3）输注胆盐：去氢胆酸钠或牛磺胆酸钠期间。在禁食组中，胆汁流量和胆汁盐排泄（以全肝为基础）分别下降了49%和41%；溴磺酞钠（BSP）和二溴磺酞钠（DBSP）的转运最大值（Tm）分别降低了59%和50%；然而，孟加拉玫瑰红（RB）的Tm保持正常。苯巴比妥预处理使BSP和DBSP的Tm分别增加了44%和29%，而RB的Tm保持不变。输注去氢胆酸盐使BSP和DBSP的Tm分别增加了27%和49%，而RB的Tm增加了12%。相反，等摩尔输注牛磺胆酸盐使RB的Tm增加幅度（56%）比BSP和DBSP更大（分别为31%和22%）。提示RB与前两种分子的肝-胆汁排泄途径不同。我们的结果强调了预测外来化合物胆汁排泄的困难，即使它们的结构非常相似。
