一种来自乌苏里叶下珠的脯氨酰内肽酶抑制性抗氧化剂。

A prolyl endopeptidase-inhibiting antioxidant from Phyllanthus ussurensis.

作者信息

Chung Shin-Kyo, Nam Ji-Ae, Jeon So-Young, Kim Sang-In, Lee Hee-Ju, Chung Tai Ho, Song Kyung-Sik

机构信息

Department of Food Technology, College of Agriculture and Life Sciences, Kyungpook National University, 1370 Sankyuk-Dong, Daegu 702-701, Korea.

出版信息

Arch Pharm Res. 2003 Dec;26(12):1024-8. doi: 10.1007/BF02994753.

DOI:10.1007/BF02994753

PMID:14723335

Abstract

A prolyl endopeptidase inhibitor was isolated from the ethyl acetate soluble fraction of Phyllanthus ussurensis. The active compound was identified as an ellagitannin, corilagin. It was shown to non-competitively inhibit prolyl endopeptidase (PEP) with the IC50 value of 1.17x10(-6) microM. The Ki value was 6.70x10(-7) M. Corilagin was less inhibitory to other serine proteases such as chymotrypsin, trypsin, and elastase, indicating that it was relatively a specific inhibitor of PEP. Corilagin also effectively inhibited reactive oxygen species such as hydroxide and superoxide anion radical, hydrogen peroxide, and DPPH. Especially, corilagin showed potent scavenging activity on the superoxide anion radical in the ESR method (IC50 = 3.79x10(-6) M) as well as xanthine oxidase system.

摘要

从乌苏里叶下珠的乙酸乙酯可溶部分分离出一种脯氨酰内肽酶抑制剂。活性化合物被鉴定为鞣花单宁，柯里拉京。结果表明，它对脯氨酰内肽酶（PEP）具有非竞争性抑制作用，IC50值为1.17×10（-6）微摩尔。Ki值为6.70×10（-7）M。柯里拉京对其他丝氨酸蛋白酶如胰凝乳蛋白酶、胰蛋白酶和弹性蛋白酶的抑制作用较小，表明它相对是PEP的特异性抑制剂。柯里拉京还能有效抑制活性氧，如氢氧根和超氧阴离子自由基、过氧化氢和DPPH。特别是，在电子自旋共振法中，柯里拉京对超氧阴离子自由基表现出强大的清除活性（IC50 = 3.79×10（-6）M），在黄嘌呤氧化酶系统中也是如此。