Abstract
Lactate dehydrogenase-C 4, (LDH-C 4) plays a central role in the metabolism of spermatogenic and mature sperm cells as well as being an enzyme which is inhibited by gossypol, a male contraceptive. Racemic and (+)-gossypol have equivalent potency as inhibitors of LDH-C 4 purified from ejaculated sperm of cynomolgus monkeys. Analogues of gossypol (gossypol-glycine ester Schiff's base, 6,6-dimethoxygossypol and ethyl gossypol) have quantitatively similar inhibitory effects on LDH-C 4 activity; apogossypol hexaacetate, however, has no inhibitory effect. Other effective inhibitors of LDH-C 4 are antimycin, naphthoquinones and lithocholic acid. LDH-C 4 may serve as a model for understanding gossypol binding domains and contraceptive action.
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