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. Author manuscript; available in PMC: 2011 Jul 8.
Published in final edited form as: J Med Chem. 2010 Jul 8;53(13):5033–5043. doi: 10.1021/jm100274c

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
a

Determined at a compound concentration of 34 μM. The compounds were not cytotoxic at this concentration in HEK-293 cells.

b

The percentage of subG1 HL-60 cells, characteristic of apoptosis. The distribution in subG1 of vehicle-treated cells was 2.2 ± 0.0%.

c

Determined at a concentration of 20 μg/mL.

d

Concentration to double the expression of QR1.

e

Determined at a compound concentration of 340 μM.