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Metabolic Fate of Oral Diethylstilbestrol in Steers

United States Department of Agriculture³

Abstract

The metabolic fate of diethylstilbestrol (DES) in steers was studied by giving single oral doses of ¹⁴C-DES and sacrificing the animals 24, 48, 72, 120, 168 and 240 hr. after dosing (two steers per time interval). Total recovery of ¹⁴C averaged 97% of the dose, with a range of 90.0 to 103.7%. Of the total ¹⁴C recovered from steers slaughtered 120 and 168 hr. after dosing, 98.5 and 99.5%, respectively, were in the excreta. For all animals, fecal excretion was two to three times that in the urine, and the gastrointestinal contents were the major reservoir of unexcreted ¹⁴C. A minimum of 85% of the ¹⁴C in feces was characterized as free DES by thin-layer chromatography (TLC). The ¹⁴C in the urine was not free DES; but after incubation with ß-glucuronidase-aryl sulfatase enzyme, a minimum of 85% was recovered as free DES (characterized by TLC). The concentrations of ¹⁴C were always higher in the liver, kidney and bile-gallbladder than in any other tissue analyzed. ¹⁴C-DES was recovered from hydrolysates of liver extracts and of bile-gallbladder extracts from several steers. Isotopic dilution procedures were the basis for these identifications. One of the liver samples from which ¹⁴C-DES was recovered came from a steer that was slaughtered 168 hr. after dosing with ¹⁴C-DES. Approximately 22% of the ¹⁴C in this liver sample was identified as ¹⁴C-DES, and this is an equivalent concentration of the order of 0.1 ppb DES. Analyses that employed gasliquid chromatography detected DES (0.9 to 1.2 ppb) in the livers from one steer slaughtered 72 hr. and another 120 hr. after ingestion of DES had ceased, but these analyses did not detect DES in livers of two steers slaughtered 168 hr. after DES ingestion had ceased.

¹ Agricultural Research Service, Metabolism and Radiation Research Laboratory, Fargo, North Dakota 58102.

² Technical assistance of B. R. Lewton is gratefully acknowledged.

³ Reference to a company or product name does not imply approval or recommendation of the product by the U.S.D.A. to the exclusion of others that may be suitable.

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