Table 3.
Influence of azo dyes 9 a–k, 15 a–h, and 20 a‐c on the deacetylase activity of human sirtuin isotypes Sirt1–3, determined by the fluorescence‐based ZMAL activity assay. Biological activity was investigated at the thermal equilibrium (Δ) and the PSS after 5 min of UV irradiation (365 nm).
|
|
Sirt1 inhibition[a] |
Sirt2 inhibition[a] |
Sirt3 inhibition[a] |
|||
|---|---|---|---|---|---|---|
|
|
Δ |
PSS [365 nm] |
Δ |
PSS [365 nm] |
Δ |
PSS [365 nm] |
|
9 a |
n.i. |
n.i. |
17 % @ 10 μm |
11 % @ 10 μm |
68 % @ 100 μm |
52 % @ 100 μm |
|
9 b |
n.i. |
n.i. |
30 % @ 10 μm |
4 % @ 10 μm |
80 % @ 100 μm |
52 % @ 100 μm |
|
9 c |
n.i. |
n.i. |
40 % @ 10 μm |
24 % @ 10 μm |
20 % @ 10 μm |
3 % @ 10 μm |
|
9 d |
n.i. |
n.i. |
44.0±9.5 μm [b] (26 % @ 10 μm) |
7.9±0.7 μm [b] (54 % @ 10 μm) |
u.i. |
u.i. |
|
9 e |
n.i. |
n.i. |
26 % @ 10 μm |
78 % @ 10 μm |
u.i. |
u.i. |
|
9 f |
n.i. |
n.i. |
46 % @ 10 μm |
65 % @ 10 μm |
u.i. |
u.i. |
|
9 g |
n.i. |
n.i. |
2.2±0.3 μm [b] |
0.9±0.2 μm [b] |
u.i. |
u.i. |
|
9 h |
n.i. |
n.i. |
27 % @ 100 μm |
52 % @ 100 μm |
n.i. |
32 % @ 100 μm |
|
9 i |
n.i. |
n.i. |
15 % @ 10 μm |
15 % @ 10 μm |
n.i. |
n.i. |
|
9 j |
n.i. |
n.i. |
80 % @ 100 μm |
59 % @ 100 μm |
u.i. |
u.i. |
|
9 k |
n.i. |
n.i. |
43 % @ 100 μm |
71 % @ 100 μm |
n.i. |
n.i. |
|
15 a |
n.i. |
7 % @ 10 μm |
6.0±1.1 μm [b] |
6.8±0.4 μm [b] |
42 % @ 10 μm |
45 % @ 10 μm |
|
15 b |
35 % @ 100 μm |
44 % @ 100 μm |
3.9±0.2 μm [b] |
6.9±0.6 μm [b] |
58 % @ 10 μm |
30 % @ 10 μm |
|
15 c |
n.i. |
6 % @ 10 μm |
0.88±0.06 μm [b] |
2.8±0.1 μm [b] |
1.1±0.2 μm [b] |
4.0±0.7 μm [b] |
|
15 d |
n.i. |
47 % @ 100 μm |
7.5±0.5 μm [b] |
8.4±0.9 μm [b] |
8.2±1.4 μm [b] |
13.0±2.2 μm [b] |
|
15 e |
n.i. |
10 % @ 10 μm |
51 % @ 10 μm |
61 % @ 10 μm |
54 % @ 10 μm |
49 % @ 10 μm |
|
15 f |
n.i. |
n.i. |
36.6±9.3 μm [b] |
1.6±0.2 μm [b] |
n.i. |
n.i. |
|
15 g |
60 % @ 100 μm |
54 % @ 100 μm |
7.2±0.5 μm [b] |
11.8±1.0 μm [b] |
64 % @ 10 μm |
22 % @ 10 μm |
|
15 h |
n.i. |
n.i. |
15.2±1.8 μm [b] |
37.5±5.2 μm [b] |
42 % @ 10 μm |
18 % @ 10 μm |
|
20 a |
n.i. |
n.i. |
0.70±0.21 μm [b] |
1.6±0.2 μm [b] |
23 % @ 10 μm |
24 % @ 10 μm |
|
20 b |
n.i. |
n.i. |
3.2±0.5 μm [b] |
6.4±0.5 μm [b] |
34 % @ 10 μm |
47 % @ 10 μm |
|
20 c |
45 % @ 100 μm |
62 % @ 100 μm |
u.i. |
6.2±0.54 μm [b] |
u.i. |
17.2±1.57 μm [b] |
[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), u.i.: unspecific interactions.