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本文用明胶玻片法研究对-羟基苯甲酸丁酯对人类精子顶体蛋白酶水解活性的抑制作用,较典型的顶体蛋白酶抑制剂TLCK 的抑制活性强20倍。应用精子尾低渗膨胀实验方法和曙红染色方法,还证明了对-羟基苯甲酸丁酯对精子膜功能有破坏作用;用不同浓度的对-羟基苯甲酸丁酯处理精子1min 后,精子尾低渗膨胀百分率与存活精子百分率具有很好的正相关性(r=0.92)。这说明此化合物的杀精子作用可能是由于对精子膜功能的损伤所致。由于这种化合物能够强烈地抑制人类精子顶体蛋白酶的蛋白水解活性。并对精子膜功能产生不可逆转的损伤,所以很有希望开发成为新型的阴道避孕药。
In this paper, gelatin slide method was used to study the inhibitory effect of p-hydroxybenzoate on human sperm acrosin proteolytic activity, 20 times stronger than the typical acrosin protease inhibitor TLCK. Using sperm tail hypoosmotic swelling test method and eosin staining method, it was also proved that para-hydroxybenzoic acid butyl had a damaging effect on sperm membrane function. After treating sperm with different concentrations of para-hydroxybenzoate for 1 min, Hypotonic swelling percentage had a good positive correlation with surviving sperm percentage (r = 0.92). This shows that the compound spermicidal effect may be due to damage to the function of the sperm membrane. Since this compound strongly inhibits the proteolytic activity of human sperm acrosin. And sperm membrane function irreversible damage, so there is great hope to develop into a new type of vaginal birth control pills.