Prenylflavonoids from Glycyrrhiza uralensis and their protein tyrosine phosphatase-1B inhibitory activities

被引：75

作者：

Li, Songpei ^{[1
]}

Li, Wei ^{[1
]}

Wang, Yinghua ^{[2
]}

Asada, Yoshihisa ^{[3
]}

Koike, Kazuo ^{[1
]}

机构：

[1] Toho Univ, Fac Pharmaceut Sci, Chiba 2748510, Japan

[2] Ningxia Inst Drug Control, Yinchuan 750004, Peoples R China

[3] Tokyo Univ Sci, Fac Pharmaceut Sci, Chiba 2788510, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 18期

关键词：

Glycyrrhiza uralensis; Flavonoids; Protein tyrosine phosphatase-1B; SIGNAL-TRANSDUCTION; CONSTITUENTS; LICORICE; OBESITY; PTP1B; ACTS;

D O I：

10.1016/j.bmcl.2010.07.110

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Two new 2-arylbenzofurans, glycybenzofuran (1) and cyclolicocoumarone (2), together with 10 known flavonoids including licocoumarone (3), glycyrrhisoflavone (4), glisoflavone (5), cycloglycyrrhisoflavone (6), isoliquiritigenin (7), licoflavone A (8), apigenin (9), isokaempferide (10), glycycoumarin (11), and isoglycycoumarin (12), were isolated from the roots of Glycyrrhiza uralensis and their structures were determined by extensive spectroscopic analyses. Compounds 1 and 5 showed significant protein tyrosine phosphatase-1B (PTP1B) inhibitory activity in vitro with the IC50 values of 25.5 and 27.9 mu M, respectively. The structure-activity relationship indicated that the presence of prenyl group and ortho-hydroxy group is important for exhibiting the activity. Kinetic analysis indicated that compound 1 inhibits PTP1B by a competitive mode, whereas compound 5 by a mixed mode. (c) 2010 Elsevier Ltd. All rights reserved.

引用

页码：5398 / 5401

页数：4

共 20 条

[1] Review of pharmacological effects of Glycyrrhiza sp and its bioactive compounds [J].