Inhibition of protein tyrosine phosphatase 1B by ursane-type triterpenes isolated from Symplocos paniculata

被引：74

作者：

Na, M ^{[1
]}

Yang, S ^{[1
]}

He, L ^{[1
]}

Oh, H ^{[1
]}

Kim, BS ^{[1
]}

Oh, WK ^{[1
]}

Kim, BY ^{[1
]}

Ahn, JS ^{[1
]}

机构：

[1] Korea Res Inst Biosci & Biotechnol, Taejon 305333, South Korea

来源：

PLANTA MEDICA | 2006年 / 72卷 / 03期

关键词：

D O I：

10.1055/s-2005-873194

中图分类号：

Q94 [植物学];

学科分类号：

071001 ;

摘要：

Inhibition of protein tyrosine phosphatase 1B (PTP1B) has been proposed as a therapy for treatment of type 2 diabetes and obesity. Bioassay-guided fractionation of the MeOH extract of the leaves and stems of Symplocos paniculata (Thunb.) Miq. (Symplocaceae), using all in vitro PTP1B inhibitory assay, resulted in the isolation of three ursane-type triterpenes, ursolic acid (1), corosolic acid (2) and 2 alpha,3 alpha,19 alpha,23-tetrahydroxyurs-12-en-28-oic acid (3). Compounds 1-3 inhibited PTP1B with IC50 values of 3.8 +/- 0.5, 7.2 +/- 0.8 and 42.1 +/- 1.5 mu M, respectively. Kinetic Studies suggest that 1 is a competitive inhibitor with a K-i value of 2.0 mu M, whereas 2 is a mixed-type inhibitor of PTP1B. Our results indicate that the Substitution of hydroxy groups on the Ursane-type triterpenes is responsible for the loss of activity, and thus 1 and 2 possessing only one or two hydroxy groups can be potential PTP1B inhibitors.

引用

页码：261 / 263

页数：3

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