IC50 Inhibition of COX-2 activity by NSAIDs
| Triflusal | Aspirin | HTB | Salicylate | Indomethacin | NS-398 | |
|---|---|---|---|---|---|---|
| μM | ||||||
| Human blood | 160 ± 10 | 180 ± 50 | 390 ± 90 | >5000 | 0.78 ± 0.03 | 0.12 ± 0.04 |
| Purified COX-2 | 280 ± 40 | 420 ± 80 | >10000 | >10000 | 0.98 ± 0.06 | 0.042 ± 0.003 |
Heparinized whole human blood was incubated at 37°C with compound or vehicle in presence of LPS (10 μg/ml) for 24 h. Activity was determined measuring the PGE2 released in the medium. Inhibition of purified COX-2 from sheep placenta (Cayman Chemical Co.) was determined spectrophotometrically. The enzyme (30–40 U) was preincubated at 37°C for 7 min. with triflusal, aspirin, HTB, and salicylate or for 2 min with indomethacin and NS-398 before activity determination. Results are mean ± S.D. (n = 3).