16-Hydroxylation of Estrone-3-Sulfate and Estrone in the Guinea Pig in Vivo*

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Abstract
[6,7-3H]Estrone-3-sulfate or [6,7-3H]-estrone of high specific activity was injected into adult female English Shorthair guinea pigs. Blood, liver, kidney, gall bladder bile and urine were obtained and investigated for metabolites. Chromatographic procedures followed by enzymatic or solvolytic cleavage of conjugates and subsequent crystallization with appropriate carrier steroids revealed the pattern of metabolites formed. Injected estrone sulfate was partially hydrolyzed and reconjugated, resulting in the production of estrone and estradiol glucuronides. The main metabolites were monosulfates of 16.alpha.-hydroxyestrone, 16-keto-17.beta.-estradiol and estriol as well as disulfates of 16.alpha.-hydroxyestrone, estriol and 16.beta.-hydroxyestrone. Particularly high amounts of these were found in urine. The main metabolites of injected estrone were glucuronides of estrone and estradiol, although the pattern of mono- and disulfated steroids was qualitatively similar to that found after estrone sulfate injection. The guinea pigs employed in the study hydroxylated estrogen in the 16.alpha.- and 16.beta.-configurations and this activity was much more pronounced after injection of estrone sulfate than after estrone.