来自绿茶的脯氨酰内肽酶抑制剂。

Prolyl endopeptidase inhibitors from green tea.

作者信息

Kim J H, Kim S I, Song K S

机构信息

Dept. of Agricultural Chemistry, College of Agriculture, Kyungpook National University, Taegu, Korea.

出版信息

Arch Pharm Res. 2001 Aug;24(4):292-6. doi: 10.1007/BF02975094.

DOI:10.1007/BF02975094

PMID:11534759

Abstract

Three prolyl endopeptidase (PEP) inhibitors were isolated from the methanolic extract of green tea leaves. They were identified as (-)-epigallocatechin gallate, (-)-epicatechin gallate, and (+)-gallocatechin gallate with the IC50 values of 1.42 x 10(-4) mM, 1.02 x 10(-2) mM, and 1.09 x 10(-4) mM, respectively. They were non-competitive with a substrate in Dixon plots and did not show any significant effects against other serine proteases such as elastase, trypsin, and chymotrypsin, suggesting that they were relatively specific inhibitors against PEP. The isolated compounds are expected to be useful for preventing and curing of Alzheimer's disease.

摘要

从绿茶叶的甲醇提取物中分离出三种脯氨酰内肽酶（PEP）抑制剂。它们被鉴定为（-）-表没食子儿茶素没食子酸酯、（-）-表儿茶素没食子酸酯和（+）-没食子儿茶素没食子酸酯，IC50值分别为1.42×10⁻⁴ mM、1.02×10⁻² mM和1.09×10⁻⁴ mM。在迪克森图中，它们与底物无竞争性，对其他丝氨酸蛋白酶如弹性蛋白酶、胰蛋白酶和胰凝乳蛋白酶没有显著影响，这表明它们是相对特异性的PEP抑制剂。预期分离出的化合物可用于预防和治疗阿尔茨海默病。