Table 2.
Influence of stilbenoid lead 3 and 6 f, 7 a–f, 11, 12 a–d, and 20 d on the deacetylase activity of human sirtuin isotypes Sirt1–3 determined in the fluorescence‐based ZMAL activity assay.
|
|
Sirt1 inhibition[a] |
Sirt2 inhibition[a] |
Sirt3 inhibition[a] |
|---|---|---|---|
|
3 |
27 % @ 50 μm |
24.6±2.8 μm [b] |
41.7±2.0 μm [b] |
|
6 f |
n.i. |
n.i. |
n.i. |
|
7 a |
14 % @ 50 μm |
7.9±0.6 μm [b] |
9.5±0.9 μm [b] |
|
7 b |
19 % @ 50 μm |
10.8±0.6 μm [b] |
7.9±0.5 μm [b] |
|
7 c |
n.i. |
55 % @ 10 μm |
64 % @ 10 μm |
|
7 d |
10 % @ 10 μm |
62 % 10 μm |
39 % @ 50 μm |
|
7 e |
17 % @ 10 μm |
54 % @ 10 μm |
66 % @ 10 μm |
|
7 f |
47 % @ 100 μm |
5.8±0.7 μm [b] |
9.4±0.7 μm [b] |
|
11 |
n.i. |
n.i. |
n.i. |
|
12 a |
33 % @ 100 μm |
45 % @ 100 μm |
45 % @ 100 μm |
|
12 b |
n.i. |
16 % @ 10 μm |
11 % @ 10 μm |
|
12 c |
n.i. |
17 % @ 10 μm |
11 % @ 10 μm |
|
12 d |
n.i. |
43 % @ 100 μm |
43 % @ 100 μm |
|
20 d |
n.i. |
49 % @ 10 μm |
33 % @ 10 μm |
[a] Percent inhibition relative to controls at the indicated concentration, [b] IC50 values (μm) with statistical limits; values are mean±SD of duplicate experiments, n.i.: no inhibition detected (<30 % @ 100 μm).