Inhibition of oCOX-1 and oCOX-2 enzymatic activities by aspirin, NCX 4016, and its analog/metabolites
Drugs were incubated with the purified enzymes for 15 min before starting the enzymatic reaction.
oCOX-1 | oCOX-2 | ||
|---|---|---|---|
| % Inhibition | |||
| Aspirin 100 μM | 94.1 ± 2.0 | 59.7 ± 1.3 | |
| Aspirin 300 μM | 99.7 ± 1.5 | 62.6 ± 1.0 | |
| NCX 4016 100 μM | 72.7 ± 0.8 | 96 ± 2.1 | |
| NCX 4016 300 μM | 97.4 ± 1.2 | 99.8 ± 1.0 | |
| NCX 4017 100 μM | 36.5 ± 1.0 | 49.5 ± 1.8 | |
| NCX 4017 300 μM | 50.8 ± 0.4 | 73.7 ± 2.5 | |
| NCX 4215 100 μM | 64.8 ± 1.5 | 42.1 ± 1.3 | |
| NCX 4215 300 μM | 79.7 ± 1.9 | 73 ± 1.9 | |
| NCX 4019 100 μM | 2.2 ± 0.4 | 1.3 ± 0.5 | |
| NCX 4019 300 μM | 3.8 ± 0.7 | 11.5 ± 1.6 | |
| NCX 4023 100 μM | 4.4 ± 0.5 | 1.8 ± 0.6 | |
| NCX 4023 300 μM | 10.6 ± 0.8 | 16.8 ± 1.3 | |
| NCX 4015 100 μM | 1.2 ± 0.1 | 1.0 ± 0.1 | |
| NCX 4015 300 μM | 1.3 ± 0.1 | 1.1 ± 0.1 | |