Evaluation of the effect of butyl p-hydroxybenzoate on the proteolytic activity and membrane function of human spermatozoa.
The inhibition of the proteolytic activity of acrosin in human spermatozoa by butyl p-hydroxybenzoate was assessed by the gelatin substrate film method. Compared with a typical acrosin inhibitor, TLCK, the inhibitory activity of butyl p-hydroxybenzoate to acrosin was much more effective (20 times) than that of TLCK, proving that butyl p-hydroxybenzoate was a potent acrosin inhibitor. The effect of butyl p-hydroxybenzoate on membrane function of human spermatozoa was evaluated using a sperm-tail hypoosmotic swelling test and supravital stain method. A good correlation (r = 0.92) was observed between the % spermatozoa with normal membrane function and the % live spermatozoa after treatment of the spermatozoa with butyl p-hydroxybenzoate for 1 min, indicating that the death of spermatozoa caused by butyl p-hydroxybenzoate is probably due to impairment of sperm membrane function. Both the inhibitory effect on acrosin and the adverse effect on membrane function suggest that butyl p-hydroxybenzoate could be developed as a new vaginal contraceptive.
Song
B L
BL
Family Planning Research Institute of Tianjin, P.R. China.
Peng
D R
DR
Li
H Y
HY
Zhang
G H
GH
Zhang
J
J
Li
K L
KL
Zhao
Y Q
YQ
D000176:Acrosin / Q000037:antagonists & inhibitors; D002462:Cell Membrane / Q000187:drug effects* / Q000502:physiology; D006801:Humans; D008297:Male; D010226:Parabens / Q000494:pharmacology*; D011480:Protease Inhibitors / Q000494:pharmacology*; D013081:Sperm Motility / Q000187:drug effects; D013094:Spermatozoa / Q000187:drug effects* / Q000378:metabolism; D014107:Tosyllysine Chloromethyl Ketone / Q000494:pharmacology
D010226:Parabens; D011480:Protease Inhibitors; D014107:Tosyllysine Chloromethyl Ketone; C038091:butylparaben; D000176:Acrosin