Table 10.
Inhibition data of human CA isoforms hCA I, II, IV, VII and XII with flavonoids 59, 63, 66, 74, 75, 76–88 reported here and the standard sulfonamide inhibitor acetazolamide (AAZ) by a stopped flow CO2 hydrase assay.
| Entry | Name | KI (nM) a | ||||
|---|---|---|---|---|---|---|
| hCA I | hCA II | hCA IV | hCA VII | hCA XII | ||
| 79 | Chrysin | >10,000 | >10,000 | 537.75 | 171.41 | 34.7 |
| 61 | Luteolin | >10,000 | 3691.6 | 293.0 b | 4.7 | 60.3 |
| 80 | Galangin | >10,000 | >10,000 | 568.3 | 24.5 | 41.8 |
| 65 | Kaempferol | >10,000 | 9525.7 | >10,000 | 25 | 145.9 |
| 67 | Isorhamnetin | >10,000 | >10,000 | 212.9 | 4.4 | 54.9 |
| 81 | Naringenin | >10,000 | >10,000 | 79.5 | 4.3 | 44.3 |
| 82 | Eriodictyol | >10,000 | >10,000 | 72.8 | 4.3 | 31.1 |
| 83 | Hesperitin | >10,000 | >10,000 | 102.1 | 3.3 | 454.1 |
| 76 | Taxifolin | >10,000 | >10,000 | 9098.2 | 493.1 | 32.5 |
| 84 | Daidzein | >10,000 | >10,000 | 718.7 | 4.2 | 56.4 |
| 85 | Biochanin A | >10,000 | >10000 | 7078.5 | 371.5 | 52.5 |
| 86 | Puerarin | >10,000 | >10,000 | >10,000 | 452.6 | 515.0 |
| 77 | Quercetin-3-O-glucoside | >10,000 | 6211.2 | 75.7 | 3.8 | 52.1 |
| 87 | Quercetin-3-O-rhamnoside | >10,000 | 6367.7 | 67.3 | 3.9 | 43.5 |
| 88 | Kaempferol-3-O-glucoside | >10,000 | 168.0 | 5591.2 | 423.7 | 4.9 |
| 89 | Tiliroside | >10,000 | >10,000 | 5468.7 | 4.6 | 134.3 |
| 90 | Kaempferol-3-O-(2″,6″-di-E-p-coumaroyl)-β-glucopyranoside | >10,000 | 8790.2 | 344.2 | 4.7 | 408.9 |
| 91 | Kaempferol-3-O-(3″,4″-diacetyl-2″,6″-di-E-p-coumaroyl)-β-glucopyranoside | >10,000 | 6863.3 | 62.2 | 26.6 | 399.7 |
| AAZ | 250 | 12 | 74 | 2.5 | 5.7 | |
a Mean from three different assays, errors were in the range of ± 5%–10% of the reported values. b From Ref. [65].