Antifertility and endocrine activities of gossypol in rodents.

Reversible male antifertility activity was obtained with orally administered gossypol acetic acid in rats at 20 mg/kg/day and in hamsters at 10 mg/kg/day but not in mice at dosages up to 40 mg/kg/day. An increased number of degenerating spermatocytes was found in the testicular tubular lumens of rats. Pigment-laden cells containing an intracytoplasmic lipofuscin-like material were noted in the testis and epididymal interstitium in rats and mice. Gossypol was also tested in the female for effects on ovulation and pregnancy. Gossypol did not inhibit ovulation in the rat at dosages up to 80 mg/kg/day but did cause 90% inhibition of pregnancy in mice treated with 80 mg/kg/day during the first two weeks of pregnancy. In several standard endocrine bioassays, gossypol did not demonstrate estrogenic, antiestrogenic, androgenic or antiandrogenic activities, but it did potentiate the androgenicity of methyltestosterone.