Schwenk M, Burr R, Pfaff E
Naunyn Schmiedebergs Arch Pharmacol. 1976 Oct;295(1):99-102. doi: 10.1007/BF00509780.
The initial rates of BSP uptake by isolated hepatocytes were compared in cells of good and poor viability. Cells with impaired viability were obtained by ageing or by accident also in fresh preparations. Viability was judged by trypan blue stainability, membrane potential and respiratory parameters indicative for energy state, substrate supply and plasma membrane permeability changes. It was found that concomitant with impaired viability there was a decline of uptake rates at low and an increase at high BSP concentrations with a crossover point at 10 muM as manifest in an increase of Km and V. Simultaneously, the affinity and size of the membrane bound fraction decreases. The results give kinetic support to the supposition that it is the decreased uptake from plasma to liver that is responsible for the prolonged plasma retention times in the liver function test of patients with impaired hepatobiliary function.
在活力良好和活力较差的分离肝细胞中比较了BSP摄取的初始速率。在新鲜制剂中，活力受损的细胞也可通过老化或偶然获得。通过台盼蓝染色性、膜电位以及指示能量状态、底物供应和质膜通透性变化的呼吸参数来判断活力。结果发现，随着活力受损，在低BSP浓度下摄取速率下降，在高BSP浓度下摄取速率增加，交叉点在10μM，表现为Km和V增加。同时，膜结合部分的亲和力和大小降低。这些结果为以下假设提供了动力学支持，即在肝胆功能受损患者的肝功能试验中，血浆向肝脏摄取减少是导致血浆滞留时间延长的原因。
