Expression of recombinant human cyclooxygenase isoenzymes in transfected COS-7 cells in vitro and inhibition by tenoxicam, indomethacin and aspirin

Prostaglandins, Leukotrienes, and Essential Fatty Acids
M LoraArtur José de Brum-Fernandes

Abstract

The recent discovery of cyclooxygenase-2 (COX-2), an isoenzyme associated mainly with inflammation created the need to reevaluate cyclooxygenase inhibitors with reliable screening methods. In the present study we standardized a technique to determine the IC50S of cyclooxygenase inhibitors on recombinant human COX-1 and COX-2 expressed in mammalian cells and used it to study the compounds tenoxicam, aspirin and indomethacin. The IC50S of aspirin, indomethacin and tenoxicam for human COX-1 were 0.41 +/- 0.07 microgram/ml, 0.008 +/- 0.003 microgram/ml, and 7.94 +/- 3.28 micrograms/ml, respectively, and for human COX-20.64 +/- 0.16 microgram/ml, 0.09 +/- 0.05 microgram/ml, and 10.61 +/- 1.50 micrograms/ml, for aspirin, indomethacin, and tenoxicam. Tenoxicam had the lowest IC50hCOX-2/IC50hCOX-1 ratio (1.34), followed by aspirin (1.53) and indomethacin (10.82). The system described in the present study provides a simple and efficient way to determine the specificity of NSAID inhibition for each of the human cyclooxygenase isoenzymes separately.

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Citations

Apr 24, 1999·The Biochemical Journal·J K GierseP C Isakson
Nov 11, 2005·Inflammopharmacology·Alessandra GamberoJosé Pedrazzoli
Nov 11, 2008·Chemico-biological Interactions·Izet M KapetanovicAlexander Lyubimov
Feb 9, 2007·Life Sciences·Jarbas Mota SiqueiraRosa Maria Ribeiro-do-Valle
Feb 1, 2014·Biochimica Et Biophysica Acta·Mary Clare CathcartGraham P Pidgeon
Jul 11, 2018·Environmental Science and Pollution Research International·Tamer I M RagabWafaa A Helmy
Oct 3, 1998·Prostaglandins, Leukotrienes, and Essential Fatty Acids·M LoraA J de Brum-Fernandes

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