@article{APS8293,
author = {Xiao-hong CHEN and Jin-ye BAI and Fang SHEN and Ai-ping BAI and Zong-ru GUO and Gui-fang CHENG},
title = {Imrecoxib: a novel and selective cyclooxygenase 2 inhibitor with anti-inflammatory effect},
journal = {Acta Pharmacologica Sinica},
volume = {25},
number = {7},
year = {2016},
keywords = {},
abstract = {AIM:
To investigate the inhibitory effect of imrecoxib, a synthetic compound of completely new structure, on cyclooxygenase 1 (COX-1) and 2 (COX-2) and its anti-inflammatory effect in vivo.
METHODS:
The inhibitory effects of imrecoxib on cyclooxygenase 1 and 2 were studied using whole cell assay with murine peritoneal macrophages induced by calcimycin and LPS. The inhibitory effects of imrecoxib on mRNA level of COX-1 and COX-2 in human macrophage cell line U937 were detected by reverse transcription polymerase chain reaction (RT-PCR) analysis. Effects of imrecoxib on acute and chronic inflammation were evaluated in rat carrageenan induced edema model and rat adjuvant-induced arthritis model, respectively.
RESULTS:
Imrecoxib was found to inhibit COX-1 and COX-2 with IC50 value of 115+/-28 nmol/L and 18+/-4 nmol/L, respectively. Imrecoxib was shown to selectively and dose-dependently inhibit COX-2 mRNA level. Imrecoxib effectively inhibited carrageenan-induced acute inflammation at the doses of 5, 10, and 20 mg/kg i.g. and adjuvant-induced chronic inflammation at the doses of 10 and 20 mg/kg/d i.g.
CONCLUSION:
Imrecoxib is a novel and moderately selective COX-2 inhibitor that possesses anti-inflammatory effect by inhibition of COX-2 mRNA expression.},
issn = {1745-7254}, url = {http://www.chinaphar.com/article/view/8293}
}