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

AbstractAIM:
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.
AuthorsXiao-hong Chen, Jin-ye Bai, Fang Shen, Ai-ping Bai, Zong-ru Guo, Gui-fang Cheng
JournalActa pharmacologica Sinica (Acta Pharmacol Sin) Vol. 25 Issue 7 Pg. 927-31 (Jul 2004) ISSN: 1671-4083 [Print] United States
PMID15210067 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Anti-Inflammatory Agents, Non-Steroidal
  • Cyclooxygenase 2 Inhibitors
  • Cyclooxygenase Inhibitors
  • Imrecoxib
  • Isoenzymes
  • Membrane Proteins
  • Pyrroles
  • RNA, Messenger
  • Sulfides
  • Cyclooxygenase 1
  • Cyclooxygenase 2
  • PTGS1 protein, human
  • PTGS2 protein, human
  • Prostaglandin-Endoperoxide Synthases
  • Ptgs1 protein, mouse
  • Ptgs1 protein, rat
Topics
  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal (pharmacology)
  • Arthritis, Experimental (pathology)
  • Cyclooxygenase 1
  • Cyclooxygenase 2
  • Cyclooxygenase 2 Inhibitors
  • Cyclooxygenase Inhibitors (pharmacology)
  • Edema (pathology)
  • Humans
  • Isoenzymes (antagonists & inhibitors, biosynthesis, genetics)
  • Male
  • Membrane Proteins
  • Mice
  • Mice, Inbred C57BL
  • Prostaglandin-Endoperoxide Synthases (biosynthesis, genetics)
  • Pyrroles (chemical synthesis, pharmacology)
  • RNA, Messenger (genetics)
  • Rats
  • Rats, Wistar
  • Sulfides (chemical synthesis, pharmacology)
  • U937 Cells

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