Hydrolysis of phospholipid monolayers by human spermatozoa. Inhibition by male contraceptive gossypol.
Monomolecular films of phospholipid were used to study the interaction of intact human spermatozoa with model membranes. Exclusively with negatively charged phosphatidylglycerol monolayers rapid penetration of spermatozoa into the monolayer with subsequent hydrolysis of the lipid was triggered by the addition of 5 mM calcium into the medium. The results suggest the localization of a calcium-dependent phospholipase A2 at the outer acrosomal or plasma membrane of human spermatozoa with its active site exposed to the external environment. Preincubation of the cells with 100 microM gossypol completely abolished the ability of human spermatozoa to hydrolyze or penetrate monolayers of phosphatidylglycerol. The inhibition of the phospholipase activity by gossypol may contribute to the unknown contraceptive mechanisms of this non-steroidal male antifertility agent.
D006072:Gossypol / Q000494:pharmacology*; D006801:Humans; D006868:Hydrolysis; D008297:Male; D008563:Membrane Lipids / Q000378:metabolism*; D008567:Membranes, Artificial; D010740:Phospholipases / Q000037:antagonists & inhibitors; D010743:Phospholipids / Q000378:metabolism*; D013094:Spermatozoa / Q000187:drug effects* / Q000378:metabolism
D008563:Membrane Lipids; D008567:Membranes, Artificial; D010743:Phospholipids; D010740:Phospholipases; D006072:Gossypol