[南德希：一种强大的人类顶体蛋白酶活性抑制剂]

[Nandeshi: a powerful inhibitor of human acrosin activity].

作者信息

Song Gui-Hong, Zhang Jue, Zhang Xiao-Meng, Ning Wei-Wei, Ji Ya-Zhong, Hui Ning, Zhao Ya-Nan, Zhou You-Jun, Zhu Ju, Lü Jia-Guo

机构信息

Research Center of Reproductive Medicine, Changhai Hospital, 2. School of Pharmacology, The Second Military, Shanghai 200433, China.

出版信息

Zhonghua Nan Ke Xue. 2009 Aug;15(8):700-2.

PMID:19852269

Abstract

OBJECTIVE

To evaluate the inhibitory effect of Nandeshi, an acrosin inhibitor, on human acrosin activity.

METHODS

We collected sperm samples from 10 healthy fertile men and cultured them with Nandeshi at 30 degrees C for 5 minutes at the concentrations of 0. 100, 0.120, 0.144, 0.173, 0.207, 0.249, 0.299, 0.358 and 0.430 mmol/L, with the controls treated with a well-known acrosin inhibitor N-alpha-p-tosyl-L-lysine chloromethylketone (TLCK) at 150.0, 189.8, 213.6, 240.3, 270.3, 304.1 and 342.1 mmol/L. Then we determined the residual activity of human acrosin by improved Kennedy assay.

RESULTS

The residual activity of acrosin was negatively correlated with the Nandeshi concentration, and Nandeshi exhibited an inhibition rate about 800 times that of TLCK.

CONCLUSION

Nandeshi has a powerful inhibitory effect on human acrosin, and improved Kennedy assay is a simple, practical and highly sensitive technique for the detection of human acrosin activity.

摘要

目的

评估顶体蛋白酶抑制剂南德士对人顶体蛋白酶活性的抑制作用。

方法

我们收集了10名健康有生育能力男性的精液样本，并将其与南德士在30℃下分别以0.100、0.120、0.144、0.173、0.207、0.249、0.299、0.358和0.430 mmol/L的浓度培养5分钟，对照组则用著名的顶体蛋白酶抑制剂N-α-对甲苯磺酰-L-赖氨酸氯甲基酮（TLCK）在150.0、189.8、213.6、240.3、270.3、304.1和342.1 mmol/L的浓度进行处理。然后我们通过改良的肯尼迪试验测定人顶体蛋白酶的残余活性。