Stanczyk F Z, Solomon S
Steroids. 1978 May;31(5):627-43. doi: 10.1016/s0039-128x(78)80003-8.
A mixture of 3H-15alpha-hydroxyandrostenedione and 14C-15alpha-hydroxydehydroisoandrosterone was injected intravenously into two subjects in the third trimester of pregnancy and, in a second study, directly into two fetuses in utero during transfusion for erythroblastosis fetalis. The urine was collected for 4-5 days and steroid conjugates in the urine were hydrolyzed into sulfate and glucosiduronate fractions. From the glucosiduronate fraction 15alpha-hydroxyestriol, 15alpha-hydroxyestradiol, 15alpha-hydroxyandrostenedione and 15alpha-hydroxydehydroisoandrosterone were isolated. No metabolites were identified in the sulfate fraction of the urine. A marked difference was observed in the metabolism of 15alpha-hydroxyandrostenedione and 15alpha-hydroxydehydroisoandrosterone which is dependent on the route of administration of the substrates. Both substrates were converted to 15alpha-hydroxyestriol and 15alpha-hydroxyestradiol, and the 3H/14C ratios and percentage conversions suggest that 15alpha-hydroxyandrostenedione seems to be a better precursor of the urinary 15alpha-hydroxylated estrogens than 15alpha-hydroxydehydroisoandrosterone. The 3H/14C ratios also suggest that 15alpha-hydroxydehydroisoandrosterone was converted to 15alpha-hydroxyestriol via 15alpha-hydroxyandrostenedione, and that the formation of 15alpha-hydroxyestradiol from 15alpha-hydroxydehydroisoandrosterone via 15alpha-hydroxyandrostenedione is a pathway of minor importance. Finally, 15alpha-hydroxydehydroisoandrosterone was recovered from the urine only when the precursors were injected into the maternal circulation. Also, an unknown metabolite containing only 14C was detected in the glucosiduronate fraction of the urine of each subject.
将3H-15α-羟基雄烯二酮和14C-15α-羟基脱氢异雄酮的混合物静脉注射给两名处于妊娠晚期的受试者，在第二项研究中，在对胎儿成红细胞增多症进行输血期间，将其直接注射到两名子宫内的胎儿体内。收集尿液4至5天，并将尿液中的类固醇结合物水解为硫酸盐和葡萄糖醛酸酯部分。从葡萄糖醛酸酯部分中分离出15α-羟基雌三醇、15α-羟基雌二醇、15α-羟基雄烯二酮和15α-羟基脱氢异雄酮。在尿液的硫酸盐部分未鉴定出代谢物。观察到15α-羟基雄烯二酮和15α-羟基脱氢异雄酮的代谢存在显著差异，这取决于底物的给药途径。两种底物均转化为15α-羟基雌三醇和15α-羟基雌二醇，3H/14C比率和转化率表明，15α-羟基雄烯二酮似乎比15α-羟基脱氢异雄酮更适合作为尿中15α-羟基化雌激素的前体。3H/14C比率还表明，15α-羟基脱氢异雄酮通过15α-羟基雄烯二酮转化为15α-羟基雌三醇，并且通过15α-羟基雄烯二酮由15α-羟基脱氢异雄酮形成15α-羟基雌二醇是一条次要途径。最后，只有当前体注射到母体循环中时，才能从尿液中回收15α-羟基脱氢异雄酮。此外，在每名受试者尿液的葡萄糖醛酸酯部分中检测到一种仅含14C的未知代谢物。
