Honjo H, Barua N R, Osawa Y, Kirdani R Y, Sandberg A A
J Clin Endocrinol Metab. 1976 Dec;43(6):1294-300. doi: 10.1210/jcem-43-6-1294.
Labeled estradiol-17beta (E2) was injected into one of the renal arteries of two human subjects. At the same time, an equimolar amount of differently labeled E2 was injected into a peripheral vein. The urinary metabolites were analyzed by DEAE-Sephadex A-25 column chromatography, countercurrent distribution (CCD) and enzyme hydrolyses. Identification was made by statistical analysis of data from CCD, thin layer chromatography (TLC) and co-crystallization upon admixture with authentic compounds. The major urinary metabolites were E2-17glucosiduronate (E2-17G), E2-3G and estriol-16G (E3-16G). The E2-17G was excreted immediately following injection of 14C-E2 into the renal artery of subject no. 1, at a rate which decreased gradually with time; whereas 3H-E2-17G did not appear in the urine until 5 min after injection of 3H-E2 into a peripheral vein. The excretion of 14C-E2-17G was very prominent as opposed to that of 3H-E2-17G; however, the excretion of both 14C- and 3H-E2-17G terminated within 30 min. 14C-E2-3G was excreted immediately following injection, whereas 3H-E2-3G did not appear until 5 min after the injection. Also, the excretion of 14C-E2-3G was more prominent as opposed to that of 3H-E2-3G. The excretion of these compounds was rapid in the initial 15 min after injection and then continued slowly for 1 h. On the other hand, 14C- and 3H-E2-16G appeared at 30 min after injection and the 3H/14C ratio was almost the same as that of the injected compounds. When subject no.2 was injected with the labeles reversed, the results were very similar to those described above. The results indicate that E2 is conjugated directly in the human kidney to form the 17G and 3G and excreted into the urine, whereas the conversion of E2 to E3 occurs systematically rather than in the kidney. In contrast of E3, the kidney appears to play a minor role (no more than 10% of the total E2 is involved) in the conjugation and/or metabolism of E2 in the human.
将标记的雌二醇 - 17β（E2）注入两名受试者的一条肾动脉中。同时，将等摩尔量的不同标记的E2注入外周静脉。通过DEAE - 葡聚糖A - 25柱色谱法、逆流分配（CCD）和酶水解分析尿代谢产物。通过对CCD、薄层色谱（TLC）数据以及与 authentic 化合物混合后的共结晶进行统计分析来进行鉴定。主要的尿代谢产物是E2 - 17葡萄糖醛酸苷（E2 - 17G）、E2 - 3G和雌三醇 - 16G（E3 - 16G）。在将14C - E2注入受试者1的肾动脉后，E2 - 17G立即排出，排出速率随时间逐渐降低；而在将3H - E2注入外周静脉5分钟后，3H - E2 - 17G才出现在尿液中。与3H - E2 - 17G相比，14C - E2 - 17G的排泄非常显著；然而，14C - 和3H - E2 - 17G的排泄在30分钟内终止。14C - E2 - 3G在注射后立即排出，而3H - E2 - 3G直到注射后5分钟才出现。同样，与3H - E2 - 3G相比，14C - E2 - 3G的排泄更显著。这些化合物在注射后的最初15分钟内排泄迅速，然后在1小时内缓慢持续。另一方面，14C - 和3H - E2 - 16G在注射后30分钟出现，3H/14C比值与注射化合物的比值几乎相同。当受试者2注射的标记物颠倒时，结果与上述结果非常相似。结果表明E2在人肾中直接结合形成17G和3G并排泄到尿液中，而E2向E3的转化发生在全身而非肾脏。与E3相比，肾脏在人体E2的结合和/或代谢中似乎起次要作用（涉及的E2不超过总量的10%）。
