Metabolism of 17-beta-estradiol to 17-beta-estradiol-3-glucosiduronate and 17-beta-estradiol-17-glucosiduronate by the normal human female.

Abstract

ABSTRACT 6,7-3H-17β-estradiol (estradiol) was administered intravenously into 2 normal females and orally to 2 others. Urines collected over various time intervals were analyzed for 3H-estradiol-3-glucosiduronate and 3H-estradiol-17-glucosiduronate by Amberlite resin, DEAE-Sephadex and Celite partition chromatography followed by enzyme hydrolysis, derivative formation and reverse isotope dilution. In the first 2 hr after intravenous injection urinary estradiol-17-glucosiduronate was more than 4 times greater in amount than the 3-monoglucosiduronate. Of the total estradiol-17-glucosiduronate excreted in the first 24 hr after injection, at least 96% was in the first 2 hr, whereas estradiol-3-glucosiduronate showed a gradual increase throughout the 24-hr period. After ingestion of 3H-estradiol, no firm evidence was obtained for the presence of urinary estradiol-17-glucosiduronate, whereas estradiol-3-glucosiduronate appeared to be excreted at a greater rate than following iv injection. It is concluded that b...