Evaluation of aldose reductase inhibition and docking studies of some secondary metabolites, isolated from Origanum vulgare L. ssp. hirtum

被引：33
作者：
Koukoulitsa, C [1 ]
Zika, C
Geromichalos, GD
Demopoulos, VJ
Skaltsa, H
机构：
[1] Univ Athens, Sch Pharm, Dept Pharmacognosy & Chem Nat Prod, GR-15771 Athens, Greece
[2] Univ Thessaloniki, Sch Pharm, Dept Pharmaceut Chem, Thessaloniki 54124, Greece
[3] Theagenio Canc Hosp, Symeonidio Res Ctr, Thessaloniki, Greece
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2006年 / 14卷 / 05期
关键词：
Origanum vulgare L. ssp hirtum; aldose reductase; docking; GLUE;
D O I：
10.1016/j.bmc.2005.10.013
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
Five polar constituents of Origanum vulgare L. ssp. hirtum were investigated for their ability to inhibit aldose reductase (ALR2), the first enzyme of the polyol pathway implicated in the secondary complications of diabetes. The most active compound was found to be lithospermic acid B. Caffeic acid was inactive as it showed no inhibitory activity against the enzyme. The order of the inhibitory activity of the remaining compounds was: rosmarinic acid > 12-hydroxyjasmonic acid 12-O-beta-glucopyrano side > p-menth-3-ene-1,2-diol 1-O-beta-glucopyranoside. Docking studies have been undertaken to gain insight into the binding mode of the investigated compounds at the active site of ALR2. The predicted hydrogen bonding and hydrophobic interactions may explain the observed inhibitory activity. (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码：1653 / 1659
页数：7
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