Inhibitory properties of several synthetic compounds towards human and goat acrosin, and trypsin.
Various synthetic inhibitors were tested for their inhibitory effects on highly purified human and goat acrosin. Bovine pancreatic trypsin was included for comparison. The molar concentrations causing 50% inhibition of the enzymes show that several guanidino compounds were highly active. The most active compound, ethyl-p-(6-guanidinohexanoyloxy) benzoate methane sulfonate (EGBM) produced 50% inhibition of human acrosin, goat acrosin, and trypsin at 5.0 X 10(-7), 8.4 X 10(-7), and 6.5 X 10(-7) M concentrations, respectively. Ethyl-p-guanidinobenzoate had an eightfold higher inhibitory power towards trypsin than to human sperm acrosin. Results on the Ki determinations showed that EGBM possessed the highest antiacrosin and antitrypsin properties, indicating that the compound has very good potential as an antifertility agent.
D000176:Acrosin / Q000037:antagonists & inhibitors*; D000818:Animals; D002417:Cattle; D010450:Endopeptidases; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D006041:Goats; D006801:Humans; D007700:Kinetics; D008297:Male; D010179:Pancreas / Q000201:enzymology; D011480:Protease Inhibitors; D013094:Spermatozoa / Q000201:enzymology; D013329:Structure-Activity Relationship; D014361:Trypsin Inhibitors / Q000494:pharmacology*
D004791:Enzyme Inhibitors; D011480:Protease Inhibitors; D014361:Trypsin Inhibitors; D010450:Endopeptidases; D000176:Acrosin