Gossypol inhibition of Ca++ uptake and Ca++-ATPase in human ejaculated spermatozoal plasma membrane vesicles.

Gossypol, a plant-derived polyphenolic compound known to exert contraceptive actions in men, inhibits Ca++-transport and Ca++-activated ATPase in isolated plasma membranes of ejaculated human sperm cells. It also inhibits the membrane bound Mg++- and Na+ + K+-dependent ATPases, 5'-nucleotidase and alkaline phosphatase systems. Ca++-ATPase inhibition by gossypol is non-competitive. It abolishes the discontinuity in Arrhenius expression of temperature dependence of Ca++-ATPase and increases the energy of activation. Phosphatidyl choline and Na+-deoxycholate inhibit Ca++-transport activity in the membrane vesicles. The apparent similarity of Ca++-transport inhibition by gossypol and phosphatidyl choline may indicate the possible capability of this compound to induce changes in the lipid microenvironment of the membranes, wherein the integral proteins operate. Inhibitory effect of gossypol on the plasma membrane Ca++-pump suggests that gossypol may affect sperm motility by a mechanism which is related to the structure and functions of the plasma membrane.