CC05. a novel anti-inflammatory compound, exerts its effect by inhibition of cyclooxygenase-2 activity

doi:10.1016/j.ejphar.2005.06.020

	CC05. a novel anti-inflammatory compound, exerts its effect by inhibition of cyclooxygenase-2 activity
	Yin, LL; Zhang, WY; Li, MH; Shen, JK; Zhu, XZ
刊名	EUROPEAN JOURNAL OF PHARMACOLOGY
	2005-09-27
卷号	520 期号:1-3 页码:172-178
关键词	cyclooxygenase-2 inflammation carrageenan-induced paw edema air pouch model THP-1 cell line
ISSN号	0014-2999
DOI	10.1016/j.ejphar.2005.06.020
文献子类	Article
英文摘要	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.
WOS关键词	SELECTIVE-INHIBITION ; MESSENGER-RNA ; PROSTAGLANDIN SYNTHASE ; ENZYME-ACTIVITY ; PHORBOL ESTER ; GROWTH-FACTOR ; RAT ; COX-2 ; EXPRESSION ; DRUGS
WOS研究方向	Pharmacology & Pharmacy
语种	英语
出版者	ELSEVIER SCIENCE BV
WOS记录号	WOS:000232418600022
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/273802]
专题	药物化学研究室药理学第二研究室
通讯作者	Shen, JK
作者单位	Chinese Acad Sci, Shanghai Inst Biol Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China
推荐引用方式 GB/T 7714	Yin, LL,Zhang, WY,Li, MH,et al. CC05. a novel anti-inflammatory compound, exerts its effect by inhibition of cyclooxygenase-2 activity[J]. EUROPEAN JOURNAL OF PHARMACOLOGY,2005,520(1-3):172-178.
APA	Yin, LL,Zhang, WY,Li, MH,Shen, JK,&Zhu, XZ.(2005).CC05. a novel anti-inflammatory compound, exerts its effect by inhibition of cyclooxygenase-2 activity.EUROPEAN JOURNAL OF PHARMACOLOGY,520(1-3),172-178.
MLA	Yin, LL,et al."CC05. a novel anti-inflammatory compound, exerts its effect by inhibition of cyclooxygenase-2 activity".EUROPEAN JOURNAL OF PHARMACOLOGY 520.1-3(2005):172-178.