Table 9.
Inhibition constant KI values (μM) of human carbonic anhydrase I, II, VA, IX, and XII isoforms for compounds 60, 62, 65, 68, 72–77 and acetazolamide (AZA).
| No. | KI (nM) a | ||||
|---|---|---|---|---|---|
| hCA I | hCA II | hCA VA | hCA IX | hCA XII | |
| Apigenin (60) | 4.10 | 2.70 b | 0.30 | 0.46 | 1.00 |
| Quercetin (62) | 2.95 | 0.41 | 2.82 | 2.52 | 0.38 |
| Kaempferol (65) | 3.13 | 0.31 | 0.15 | 3.57 | 2.18 |
| Isorhamnetin (67) | >10 | 0.42 | 1.92 | 0.44 | 0.29 |
| Diosmetin (72) | >10 | >10 | 2.10 | 3.39 | 0.24 |
| Eriocitrin (73) | 3.66 | 0.34 | 4.24 | 0.43 | 0.19 |
| Hesperidin (74) | 3.60 b | 2.40 b | 2.65 | 2.22 | 0.45 |
| Naringin (75) | >10 | 0.41 | 4.08 | 3.59 | 0.17 |
| Taxifolin (76) | 2.53 | 0.26 | 3.93 | 0.45 | 0.11 |
| Quercetin-3-O-glucoside (77) | >10 | 0.44 | >10 | 2.79 | 0.22 |
| AZA | 0.10 | 0.008 | 0.38 | 0.041 | 0.038 |
a From three different assays, errors ± 5%–10% of the reported value, CO2 hydrase, stopped-flow assay. b Values from Ref. [65].