Monkey lactate dehydrogenase-C4 as a model for the interaction of enzymes with gossypol

Contraception
K J WhaleyD D Hoskins

Abstract

Lactate dehydrogenase-C4 (LDH-C4) 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-C4 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 of LDH-C4 activity; apogossypol hexaacetate, however, has no inhibitory effect. Other effective inhibitors of LDH-C4 are antimycin, naphthoquinones and lithocholic acid. LDH-C4 may serve as a model for understanding gossypol binding domains and contraceptive action.

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Citations

Feb 1, 1997·American Journal of Reproductive Immunology : AJRI·G S Gupta, N Syal
Oct 1, 1989·International Journal of Peptide and Protein Research·T Strøm-HansenJ W Jaroszewski

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