Table 1. Inhibitory Effect of Compounds 1, 2, and INDO against AKR1C3, AKR1C2, COX1, and COX2 Recombinant Purified Enzymes.
| cmpd | AKR1C3 IC50 ± SE (μM) | AKR1C2 IC50 ± SE (μM) | AKR1C2/AKR1C3a | oCOX1 IC50 ± SE (μM) | hCOX2 IC50 ± SE (μM) | COX1/AKR1C3a |
|---|---|---|---|---|---|---|
| INDO | 7.35 ± 0.56 | 8.97 ± 0.22 | 1.2 | 0.10 ± 0.01 | 0.61 ± 0.09 | 0.01 |
| 1 | 0.30 ± 0.02 | 26.75 ± 2.89 | 89 | >100 (0)b | >100 (12 ± 4)b | >333 |
| 2 | 0.94 ± 0.06 | 14.25 ± 3.39 | 15 | >100 (37 ± 1)b | >100 (26 ± 2)b | >106 |
a
Ratio of IC50 value on the indicated enzymes.
b
% of inhibition ± SE at 100 μM.