Effect of ace-inhibitors, calmodulin antagonists, acetylcholine receptor blocking, and alpha receptor blocking agents on motility of human sperm.
The purpose of this study was to investigate the influence of several pharmacological compounds on the motility and velocity of washed human spermatozoa. Results were evaluated by multiple exposure photography and computer-aided picture analysis. The motility-inhibiting effect of the antifertility drug gossypol was confirmed. Gossypol proved to be a potent inhibitor of the angiotensin converting enzyme (ACE) detectable in high concentrations in seminal plasma. However, human sperm motility was not inhibited during incubation with two other specific ACE-inhibitors (captopril, enalapril). On the contrary, high concentrations of captopril even showed a slight motility-stimulating effect. These results indicate no direct involvement of ACE in the regulation of sperm motility but suggest a direct interaction of gossypol with the plasma membrane of spermatozoa. To clarify whether or not gossypol blocks membranous ion transport, the effect of well-defined ion transport blocking agents on sperm motility was investigated. It was determined that the acetylcholine receptor blocker alpha-bungarotoxin and trifluoperazine, a specific calmodulin antagonist, inhibit sperm motility completely. Since stimulation of sperm motility by captopril may be due to an alpha-mimetic action of this compound, the influence of two alpha receptor blockers (bromocriptine, lisuride) on sperm motility was studied. Although lisuride inhibited sperm motility completely, bromocriptine revealed no influence. A temporary and reversible intervention with membrane transport processes could be a suitable way to regulate human sperm motility and male fertility.
D000317:Adrenergic alpha-Antagonists / Q000494:pharmacology; D000806:Angiotensin-Converting Enzyme Inhibitors / Q000494:pharmacology*; D001692:Biological Transport / Q000187:drug effects; D001971:Bromocriptine / Q000494:pharmacology; D002038:Bungarotoxins / Q000494:pharmacology; D002147:Calmodulin / Q000037:antagonists & inhibitors; D002216:Captopril / Q000494:pharmacology; D004656:Enalapril / Q000494:pharmacology; D006072:Gossypol / Q000494:pharmacology*; D006801:Humans; D066298:In Vitro Techniques; D008090:Lisuride / Q000494:pharmacology; D008297:Male; D008566:Membranes / Q000378:metabolism; D013081:Sperm Motility / Q000187:drug effects*; D014268:Trifluoperazine / Q000494:pharmacology
D000317:Adrenergic alpha-Antagonists; D000806:Angiotensin-Converting Enzyme Inhibitors; D002038:Bungarotoxins; D002147:Calmodulin; D014268:Trifluoperazine; D001971:Bromocriptine; D004656:Enalapril; D002216:Captopril; D008090:Lisuride; D006072:Gossypol