期刊
EUROPEAN JOURNAL OF PHARMACOLOGY
卷 520, 期 1-3, 页码 172-178出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ejphar.2005.06.020
关键词
cyclooxygenase-2; inflammation; carrageenan-induced paw edema; air pouch model; THP-1 cell line
In the present study, we examined the anti-inflammation of a novel compound, 4-[5-(3-amino-4-methylphenyl)-3-(trifluoromethyl)-IHpyrazol-1-yl]benzenesulfonamide (CC05) in vitro and in vivo. In an in vitro cell-based assay, CC05 inhibited cyclooxygenase (COX)-2derived prostaglandin E-2 (PGE(2)) synthesis with an IC50 value of 0.328 +/- 0.04 mu M compared with an IC50 value of 14.34 +/- 0.05 mu M for the inhibition of COX-1-derived PGE(2) synthesis. In two in vivo rodent models, CC05 (12.5, 25 and 50 mg/kg, i.g.) is a moderate potential and selective inhibitor of COX-2. It can reduce carrageenan-induced paw edema and PGE2 production in the inflamed pouch dose-dependently without affecting the PGE(2) production in stomachs. Furthermore, CC05 had no effect on COX-2 mRNA and protein expression in phorbol 12-myristate 13-acetate (PMA)-differentiated THP-1 human macrophages stimulated with lipopolysaccharide (LPS). These results demonstrate that CC05 is a novel COX-2 inhibitor and the anti-inflammatory action is not directed towards the transcription or translation of the COX-2 gene but only to the enzymatic activity of the protein. (c) 2005 Elsevier B.V All rights reserved.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据