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Inhibition of testicular LDH-X from laboratory animals and man by gossypol and its isomers

Summary. The inhibitory effect of (+)-, (–)-, (±)-gossypol and (±)-gossypol acetic acid upon testicular cytosolic LDH-X was measured in vitro. Gossypol acetic acid (0-100 µmol/l) inhibited LDH-X prepared from the testes of the mouse > rabbit > human > rat > hamster. There was no relationship between inhibition and in-vivo antifertility activity. LDH activity measured in vitro in serum of men and hamsters was unaffected by gossypol. Gossypol and its isomers were non-competitive inhibitors of human and hamster LDH-X with respect to the coenzyme NADH, competitive inhibitors of human LDH-X and noncompetitive—competitive inhibitors of hamster LDH-X with respect to the substrate -ketobutyrate. Co-incubation with human serum albumin or poly-L-lysine but not lysine protected human and hamster LDH-X from gossypol.