Biotransformation of diethylstilbestrol in the rhesus monkey and the chimpanzee

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Abstract
Diethylstilbestrol (DES) is considered a teratogen and a transplacental carcinogen in humans. To compare its biotransformation in nonhuman primates to that in humans, a metabolic study was done in rhesus monkeys and chimpanzees. After an oral dose of 1 mg/kg [14C]DES, approximately 59% of the ingested radioactivity was found in the urine and 28% in the feces of 2 female rhesus monkeys after 4 days, while in male rhesus monkeys urinary radioactivity accounted for 43% and fecal radioactivity for 35%. In chimpanzees, 63% of a 0.5 mg/kg dose was excreted with the urine in a female and 47% in a male animal. In both species, urinary radioactivity was predominantly (> 70%) associated with glucuronides. Besides DES, 3 metabolites were found in the urinary glucuronide fraction of rhesus monkeys and chimpanzees by radio gas chromatography and were identified as dienestrol and .omega.-hydroxy derivatives of DES and dienestrol. Fecal radioactivity in rhesus monkeys consisted exclusively of DES. Glucuronidation of DES appears to occur in neonatal and fetal rhesus monkeys.

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