Table 2.
Biological Evaluation of Resveratrol and Resveratrol Sulfates in Bioassays Indicative of Cancer Chemoprevention
compound tested |
||||||
---|---|---|---|---|---|---|
assay | Resveratrol | 2 | 3 | 4 | 5 | 7 |
NFκB | ||||||
% inhibitiona | 75.7 ± 2.12 | 36.7 ± 9.4 | 53.4 ± 2.9 | 42.5 ± 5.23 | 33.0 ± 4.81 | 64.0 ± 2.26 |
IC50 (μM) | 0.173±0.05 | – | – | – | – | 18.2 ± 0.99 |
COX-1 | ||||||
% inhibitiona | 75.2 ± 4.53 | 37.8 ± 0.71 | 23.3 ± 0.98 | 30.9 ± 2.69 | 74.3 ± 0.99 | 63.2 ± 3.39 |
IC50 (μM) | 6.65 ± 2.5 | – | – | – | 3.60 ± 0.8 | 5.55 ± 1.73 |
COX-2 | ||||||
% inhibitiona | 72.2±4.67 | 2.4 ± 2.0 | 16.5 ± 2.69 | 25.5 ± 5.52 | 62.0 ± 1.7 | 65.8 ± 7.64 |
Nitric Oxide | ||||||
% inhibitiona | 71.8 ± 3.5 | 24.8 ± 3.1 | 41.7 ± 5.5 | 4.8 ± 4.5 | 41.0 ± 0.7 | 56.8 ± 5.9 |
IC50 (μM) | 15.0 ± 2.6 | – | – | – | – | – |
% SubG1a,b | 24.9 ± 0.149 | – | – | – | – | 2.22 ± 0.012 |
Cytotoxicityc | ||||||
KB % survival | 47.8 ± 5.2 | 78.1 ± 7.8 | 99.3 ± 15.0 | 84.2 ± 13.1 | 70.3 ± 8.8 | 108.5 ± 10.3 |
MCF7 % survival | 38.6 ± 3.5 | 106.7 ± 9.6 | 100.0 ± 11.3 | 97.2 ± 5.2 | 51.7 ± 0.2 | 103.4 ± 8.8 |
Aromatase | ||||||
% inhibitiona | 34.8 ± 1.21 | 28.5 ± 0.2 | 22.5 ± 0.64 | 20.5 ± 0.43 | 28.2 ± 1.12 | 30.4 ± 0.56 |
QR1 | ||||||
CD (μM)d | 21 ± 0.46 | > 11.7 | > 10.1 | > 10.1 | 2.6 ± 0.38 | > 6.9 |
DPPH | ||||||
% inhibitione | 65.2 ± 2.0 | 0.4 ± 1.1 | 6.8 ± 1.0 | 14.5 ± 4.2 | 68.0 ± 1.9 | 42.8 ± 2.5 |
IC50 (μM) | 178.5 ± 9.3 | – | – | – | 219.2 ± 3.1 | – |
Determined at a compound concentration of 34 μM. The compounds were not cytotoxic at this concentration in HEK-293 cells.
The percentage of subG1 HL-60 cells, characteristic of apoptosis. The distribution in subG1 of vehicle-treated cells was 2.2 ± 0.0%.
Determined at a concentration of 20 μg/mL.
Concentration to double the expression of QR1.
Determined at a compound concentration of 340 μM.