Cyclooxygenase (COX) and 5-lipoxygenase (5-LOX) selectivity of COX inhibitors

被引：27

作者：

Sud'ina, G. F. ^{[1
]}

Pushkareva, M. A. ^{[1
]}

Shephard, P. ^{[2
]}

Klein, T. ^{[2
]}

机构：

[1] Moscow MV Lomonosov State Univ, AN Belozersky Inst Physicochem Biol, Moscow 199991, Russia

[2] Altana Pharma AG, Dept Biochem, D-78467 Constance, Germany

来源：

PROSTAGLANDINS LEUKOTRIENES AND ESSENTIAL FATTY ACIDS | 2008年 / 78卷 / 02期

关键词：

D O I：

10.1016/j.plefa.2007.12.006

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：

In vitro evaluations of the selectivity of COX inhibitors are based on a great variety of experimental protocols. As a result, data available on cyclooxygenase (COX)-1/COX-2/5-lipoxygenase (LOX) selectivity of COX inhibitors lack consistency. We, therefore, performed a systematic analysis of the COX-1/COX-2/5-LOX selectivity of 14 compounds with selective COX inhibitory activity (Coxibs). The compounds belonged to different structural classes and were analyzed employing the well-recognized whole-blood assay. 5-LOX activity was also tested on isolated human polymorphonuclear leukocytes. Among COX inhibitors, celecoxib and ML-3000 (licofelone) inhibited 5-LOX in human neutrophils at micromolar ranges. Surprisingly, ML-3000 had no effect on 5-LOX product synthesis in whole-blood assay. In addition, we could show that inhibition of COX pathways did not increase the transformation of arachidonic acid by the 5-LOX pathway. (c) 2008 Elsevier Ltd. All rights reserved.

引用

页码：99 / 108

页数：10

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