Imrecoxib: a novel and selective cyclooxygenase 2 inhibitor with anti-inflammatory effect  

作　　者：Xiao-hongCHEN Jin-yeBAI FangSHEN Ai-pingBAI Zong-ruGUO Gui-fangCHENG 

机构地区：[1]DepartmentofPharmacology,InstituteofMateriaMedica,ChineseAcademyofMedicalSciencesandPekingUnionMedicalCollege,Beijing100050,China

出　　处：《Acta Pharmacologica Sinica》2004年第7期927-931,共5页中国药理学报（英文版）

基　　金：Project supported by National Natural Science Foundation of China (No 20072057).

摘　　要：AIM: To investigate the inhibitory effect of imrecoxib, a synthetic compoundof completely new structure, on cyclooxygenase 1 (COX-1) and 2 (COX-2) and its anti-inflammatoryeffect in vivo. METHODS: The inhibitory effects of imrecoxib on cyclooxygenase 1 and 2 were studiedusing whole cell assay with murine peritoneal mac-rophages induced by calcimycin and LPS. Theinhibitory effects of imrecoxib on mRNA level of COX-1 and COX-2 in human macrophage cell line U937were detected by reverse transcription polymerase chain reaction (RT-PCR) analysis. Effects ofimrecoxib on acute and chronic inflammation were evaluated in rat carrageenan induced edema modeland rat adjuvant-induced arthritis model, respectively. RESULTS: Imrecoxib was found to inhibitCOX-1 and COX-2 with IC_(50) value of 115+-28 nmol/L and 18+-4 nmol/L, respectively. Imrecoxib wasshown to selectively and dose-dependently inhibit COX-2 mRNA level. Imrecoxib effectively inhibitedcarrageenan-induced acute inflammation at the doses of 5, 10, and 20 mg·kg^(-1) ig andadjuvant-induced chronic inflammation at the doses of 10 and 20 mg·kg^(-1)·d^(-1) ig. CONCLUSION:Imrecoxib is a novel and moderately selective COX-2 inhibitor that possesses anti-inflammatoryeffect by inhibition of COX-2 mRNA expression.AIM: To investigate the inhibitory effect of imrecoxib, a synthetic compoundof completely new structure, on cyclooxygenase 1 (COX-1) and 2 (COX-2) and its anti-inflammatoryeffect in vivo. METHODS: The inhibitory effects of imrecoxib on cyclooxygenase 1 and 2 were studiedusing whole cell assay with murine peritoneal mac-rophages induced by calcimycin and LPS. Theinhibitory effects of imrecoxib on mRNA level of COX-1 and COX-2 in human macrophage cell line U937were detected by reverse transcription polymerase chain reaction (RT-PCR) analysis. Effects ofimrecoxib on acute and chronic inflammation were evaluated in rat carrageenan induced edema modeland rat adjuvant-induced arthritis model, respectively. RESULTS: Imrecoxib was found to inhibitCOX-1 and COX-2 with IC_(50) value of 115+-28 nmol/L and 18+-4 nmol/L, respectively. Imrecoxib wasshown to selectively and dose-dependently inhibit COX-2 mRNA level. Imrecoxib effectively inhibitedcarrageenan-induced acute inflammation at the doses of 5, 10, and 20 mg·kg^(-1) ig andadjuvant-induced chronic inflammation at the doses of 10 and 20 mg·kg^(-1)·d^(-1) ig. CONCLUSION:Imrecoxib is a novel and moderately selective COX-2 inhibitor that possesses anti-inflammatoryeffect by inhibition of COX-2 mRNA expression.

关 键 词：IMRECOXIB cyclooxygenase 1 cyclooxygenase 2 cyclooxygenase inhibitors INFLAMMATION 

分 类 号：R392[医药卫生—免疫学]