Beckmann D, Breuer H
Hoppe Seylers Z Physiol Chem. 1975 Nov;356(11):1743-51.
After incubation of [4-14C]oestrone (E1) with liver slices from minipigs, the ether-soluble fraction contained [4-14C]oestradiol-17 beta (E2). In the protein-bound fractions, only polar metabolites were found, whereas in the water-soluble fraction the 3-monoglucuronide of oestriol (E1) was the preferred conjugate. When E2 was used as a substrate, E1 was present as main metabolite in the ether-soluble fraction. The radioactive metabolites in the protein-bound and water-soluble fractions were similar to those in the experiments with E1. The metabolism of E1 and E2 was dependent on age. Thus, the rate of conversion of oestrogens was greater in liver tissue of infertile male animals than in fertile males. In contrast, the two steroids were metabolised more rapidly in liver of fertile female minipigs than in infertile female animals. In fertile animals, the metabolic pattern of oestrogens in the ether-soluble, the protein-bound and the water-soluble fractions showed sex dependence: In females, E1 and E2 were metabolised to a greater extent by liver slices than in males. On the other hand, in experiments with male minipigs, E3-3-monoglucuronide was the only metabolite in the water-soluble fraction, whereas liver slices of female animals not only form E3-3-monoglucuronide, but also the 3-glucuronides of E1 and E2. The results described here show that, in liver tissue of minipigs, the oxidoreduction of E2 and E1 is the predominant reaction; in contrast to human liver, hydroxylation reactions play only a minor role. It may be concluded that there are differences in the metabolism of steroid hormones in man and minipig.
将[4-¹⁴C]雌酮(E1)与小型猪的肝切片共同孵育后,醚溶性部分含有[4-¹⁴C]雌二醇-17β(E2)。在蛋白质结合部分,仅发现极性代谢物,而在水溶性部分,雌三醇(E3)的3-单葡萄糖醛酸苷是主要的共轭物。当使用E2作为底物时,E1作为主要代谢物存在于醚溶性部分。蛋白质结合部分和水溶性部分中的放射性代谢物与用E1进行的实验中的代谢物相似。E1和E2的代谢取决于年龄。因此,不育雄性动物肝组织中雌激素的转化速率高于可育雄性动物。相反,这两种类固醇在可育雌性小型猪肝中的代谢比不育雌性动物更快。在可育动物中,醚溶性、蛋白质结合和水溶性部分中雌激素的代谢模式显示出性别依赖性:在雌性中,E1和E2被肝切片代谢的程度比雄性更大。另一方面,在雄性小型猪的实验中,E3-3-单葡萄糖醛酸苷是水溶性部分中的唯一代谢物,而雌性动物的肝切片不仅形成E3-3-单葡萄糖醛酸苷,还形成E1和E2的3-葡萄糖醛酸苷。此处描述的结果表明,在小型猪肝组织中,E2和E1的氧化还原是主要反应;与人类肝脏不同,羟基化反应仅起次要作用。可以得出结论,人类和小型猪的类固醇激素代谢存在差异。