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AB0223 Evaluation of classical nsaids and cox-2 selective inhibitors on purified ovine enzymes and human whole blood
  1. X De Leval1,
  2. JM Dogne1,
  3. J Delarge1,
  4. JY Reginster2,
  5. Y enrotin2
  1. 1Department of Medicinal Chemistry
  2. 2Bone and Cartilage Metabolism Research Unit, Institute of Pathology, CHU Start-Tilman, Liège, Belgium

Abstract

Objectives In this study, we evaluated the cyclooxygenases (COX) inhibitory profile of NSAIDs in a cellular assay using human whole blood.

Methods Human whole blood assay was performed using fresh blood from normal volunteers. COX-1 assay: Fresh blood was collected into tubes containing no anticoagulants, vortexed and incubated at 37°C under constant agitation for 1 h to allow the blood clot. The serum was then obtained by centrifugation and was assayed for thromboxane B2 (TXB2) using a enzyme immunoassay. COX-2 assay: Fresh blood was collected in heparinized tubes and activated by treatment with lipopolysaccharide at the final concentration of 100 μg/ml. After 24 h of incubation with the drugs, plasma was collected and assayed for prostaglandin E2 (PGE2). PGE2 production was quantified by a specific radioimmunoassay. Drugs were tested at the concentrations ranged among 0.01 to 100 μmol/l.

Abstract AB0223 Table 1

Conclusion In the whole blood test and based on the IC50 values, the majority of the NSAID tested preferentially inhibits COX-2. Aceclofenac shows the best selectivity whereas indomethacin preferentially inhibited COX-1.

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