Orzes N, Bellentani S, Aldini R, Simoni P, Ferretti I, Lunazzi G C, Sottocasa G L, Tiribelli C
Clin Sci (Lond). 1985 Nov;69(5):587-93. doi: 10.1042/cs0690587.
Sex difference in the hepatic uptake of sulphobromophthalein (BSP) was investigated in male and female rats in three different experimental models. In the intact animal the BSP plasma disappearance rate was significantly higher (P less than 0.01) in females than in males when 0.15 or 1.5 mumol/kg body wt. was injected. Comparable values were found at the highest BSP dose (15 mumol/kg body wt.) used. In the perfused liver, the first-pass hepatic extraction and the uptake velocity were significantly higher (P less than 0.001) in female rats at low BSP doses (0.3-750 mumol/g of liver) whereas identical values were found at higher concentrations. In hepatocytes isolated by collagenase perfusion, the BSP uptake occurs via two different uptake sites in both sexes. The Km of the high affinity sites was lower in females than in males (3.67 +/- 0.58 vs 7.24 +/- 0.68 mumol/l, P less than 0.001) whereas Vmax. showed comparable values (2.70 +/- 0.36 vs 2.47 +/- 0.45 nmol of BSP/mg of protein, NS). In contrast, no difference was found in the kinetic parameters of the low affinity sites (Km 50.6 +/- 31.1 vs 61.0 +/- 17.5 mumol/l; Vmax. 21.9 +/- 13.2 vs 25.0 +/- 3.6 nmol of BSP/mg of protein, mean +/- SD, NS, females and males respectively). Taken together these data show that low doses of BSP are taken up by the liver more efficiently in female than in male rats and are consistent with a sex-related difference in the affinity but not in the number of the BSP high affinity uptake sites.
在三种不同的实验模型中，对雄性和雌性大鼠肝脏摄取磺溴酞钠（BSP）的性别差异进行了研究。在完整动物中，当注射0.15或1.5 μmol/kg体重的BSP时，雌性动物的BSP血浆消失率显著高于雄性（P<0.01）。在使用的最高BSP剂量（15 μmol/kg体重）时，得到了类似的值。在灌注肝脏中，低BSP剂量（0.3 - 750 μmol/g肝脏）时，雌性大鼠的首过肝脏提取率和摄取速度显著更高（P<0.001），而在较高浓度时得到了相同的值。在用胶原酶灌注分离的肝细胞中，两性的BSP摄取均通过两个不同的摄取位点发生。雌性高亲和力位点的Km低于雄性（3.67±0.58对7.24±0.68 μmol/L，P<0.001），而Vmax显示出类似的值（2.70±0.36对2.47±0.45 nmol BSP/mg蛋白质，无显著性差异）。相反，低亲和力位点的动力学参数没有差异（Km 50.6±31.1对61.0±17.5 μmol/L；Vmax 21.9±13.2对25.0±3.6 nmol BSP/mg蛋白质，平均值±标准差，无显著性差异，分别为雌性和雄性）。综合这些数据表明，低剂量的BSP在雌性大鼠肝脏中的摄取比雄性大鼠更有效，这与BSP高亲和力摄取位点的亲和力存在性别相关差异但数量无差异是一致的。
