Calcium channel antagonist verapamil modulates human spermatozoal functions.
The effect of calcium channel blocker, verapamil (0.5-50 microM), has been studied in vitro in relation to certain spermatozoal functions in human ejaculates. Disruptive changes in the head and tail region of the spermatozoa, separation of heads from tails and coiling of the tail were observed. Motility was considerably reduced, while the pattern of motility also changed from rapid, linear progression to slow or sluggish linear or non-linear movement and finally to non-progressive motility, or even immotility. Verapamil significantly inhibited the influx of extracellular Ca2+. The study of kinetic effects further revealed a reduction in the maximum uptake velocity, but no change in the apparent substrate affinity constant. A highly significant decrease in Ca(2+)-dependent ATPase activity was also noted. In order to see whether this drug had any cytotoxic effect, presumably through lipid peroxides, thiobarbituric acid-reactive substances were measured. Verapamil produced an increase in the formation and release of malonyldialdehyde. The level of membrane cholesterol and phospholipid in the spermatozoa was also lowered considerably. The potential of such a calcium channel blocking agent in the designing of a male contraceptive programme is discussed.
Anand
R J
RJ
Department of Zoology, Panjab University, Chandigarh, India.
Kanwar
U
U
Sanyal
S N
SN
D002118:Calcium / Q000378:metabolism; D002121:Calcium Channel Blockers / Q000494:pharmacology*; D000252:Calcium-Transporting ATPases / Q000378:metabolism; D006801:Humans; D050356:Lipid Metabolism; D008297:Male; D010084:Oxidation-Reduction; D013081:Sperm Motility / Q000187:drug effects; D013094:Spermatozoa / Q000187:drug effects* / Q000378:metabolism / Q000648:ultrastructure; D014700:Verapamil / Q000494:pharmacology*
D002121:Calcium Channel Blockers; D014700:Verapamil; D000252:Calcium-Transporting ATPases; D002118:Calcium