Bhattacharyya A K, Sarkar S R, Datta D
Int J Fertil. 1986 Sep-Oct;31(4):293-7.
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.
测试了各种合成抑制剂对高度纯化的人及山羊顶体蛋白酶的抑制作用。加入牛胰蛋白酶作为对照。引起酶50%抑制的摩尔浓度表明，几种胍基化合物具有高活性。活性最高的化合物，对-（6-胍基己酰氧基）苯甲酸乙酯甲磺酸盐（EGBM），分别在5.0×10⁻⁷、8.4×10⁻⁷和6.5×10⁻⁷M浓度下对人顶体蛋白酶、山羊顶体蛋白酶和胰蛋白酶产生50%的抑制作用。对-胍基苯甲酸乙酯对胰蛋白酶的抑制能力比对人精子顶体蛋白酶高八倍。关于Ki测定的结果表明，EGBM具有最高的抗顶体蛋白酶和抗胰蛋白酶特性，表明该化合物作为抗生育剂具有很好的潜力。
