对-羟基苯甲酸丁酯对人精子顶体蛋白酶的抑制作用及其对精子膜功能的影响

Evaluation of Effect of Butyl p-hydroxybenzoate on Proteolytic Activity and Membrane Function of Human Spermatozoa

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。

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 acrosininhibitor,TLCK,the inhibitory activity of butyl p-hydroxybenzoate on acrosin was much moreeffective(20 times),proving that butyl p-hydroxybenzoate was a potent acrosin inhibitor.The effectof butyl p-hydroxybenzoate on the membrane function of human spermatozoa was evaluated by asperm-tail hypo-osmotic swelling test and supravital stain method.A good correlation(r=0.92)wasobserved between the % spermatozoa with normal membrane function and the % live spermatozoaafter the treatment of the spermatozoa with butyl p-hydroxybenzoate for 1 min,indicating that thedeath of spermatozoa caused by butyl p-hydroxybenzoate is probably due to injury of spermmembrane function.The inhibitory effect on acrosin together with the injury effect on membranefunction suggests that butyl p-hydroxybenzoate could be developed as a new vaginal contraceptive.