Urinary and Biliary Excretion of 14C-Gossypol in Swine

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Abstract
The urinary and biliary excretion of 14C-labeled gossypol was studied in the pig following a single oral dose of 6.7 mg/kilogram of body weight (3.7 µCi). The resolution of urinary and biliary metabolites of gossypol was undertaken by column chromatography on DEAE-cellulose anion exchanger in the formate form. The metabolites were eluted with an increasing gradient from 0 to 0.50 M ammonium formate buffer, pH 3.5. In this scheme, eight and seven individual peaks containing radioactivity were obtained from urine and bile, respectively. The main metabolites in the urine seem to be water-soluble metabolites (42.6%), nonconjugated metabolites (27.1%), glucuronides (12.1%), hot-acid hydrolyzed metabolites (7.7%), and sulfates (7.0%). The metabolites found in pig bile consisted almost entirely of the same conjugates that occur in the urine, but the bulk of the radioactivity was due to the glucuronides (32.7%) followed by sulfuric acid conjugates (22.0%), water-soluble metabolites (21.7%), and hot-acid hydrolyzed metabolites (15.6%), with nonconjugated metabolites having the least radioactivity (6.6%).