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.
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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