In vitro COX-1 and COX-2 enzyme inhibitory activities of iridoids from Penstemon barbatus, Castilleja tenuiflora, Cresentia alata and Vitex mollis

被引：22

作者：

Angeles Ramirez-Cisneros, M. ^{[1
]}

Yolanda Rios, Maria ^{[1
]}

Berenice Aguilar-Guadarrama, A. ^{[1
]}

Rao, Praveen P. N. ^{[2
]}

Aburto-Amar, Rola ^{[3
]}

Rodriguez-Lopez, Veronica ^{[3
]}

机构：

[1] Univ Autonoma Estado Morelos, IICBA, Ctr Invest Quim, Cuernavaca 62209, Morelos, Mexico

[2] Univ Waterloo, Sch Pharm, Waterloo, ON N2L 3G1, Canada

[3] Univ Autonoma Estado Morelos, Fac Farm, Cuernavaca 62209, Morelos, Mexico

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2015年 / 25卷 / 20期

基金：

加拿大自然科学与工程研究理事会;

关键词：

Iridoids; Cyclooxygenase-2; Cyclooxygenase-1; Non-steroidal anti-inflammatory drugs; Prostaglandin; ANTIINFLAMMATORY COMPOUNDS; CYCLOOXYGENASE-2; GLUCOSIDES; INFLAMMATION; AGENTS; PLANTS;

D O I：

10.1016/j.bmcl.2015.08.075

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A group of sixteen iridoids isolated from plants used as anti-inflammatory remedies in Mexican folk medicine were evaluated for their potential to inhibit cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) enzymes. From these assays, loganic acid (10) was identified as the most promising compound with both COX-1 (36.0 +/- 0.6%) and COX-2 (80.8 +/- 4.0%) inhibition at 10 mu M. Compound 10 shows a better inhibition against the COX-2 enzyme. Other iridoids tested in the present study showed weak or no inhibition against these enzymes. Furthermore, herein are presented key interactions of iridoid 10 with COX-1 and COX-2 enzymes through molecular docking studies. These studies suggest that 10 exhibits anti-inflammatory activity due to COX inhibition. (C) 2015 Elsevier Ltd. All rights reserved.

引用

页码：4505 / 4508

页数：4

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