Determination of cell-based inhibitory activity and IC50 of test compounds and control. The cell-based inhibitory activity was estimated at 10 μM concentration in HepG2 cells against Sirt1 and; Sirt2 and Sirt3. IC50 values are calculated by enzyme inhibition assay using human recombinant Sirt1, n = 3, and the results were represented as the mean of 3 independent experimentsa.
| Comp. | % Inhibition | Sirt1 IC50 (μM) | |
|---|---|---|---|
| Sirt1 | Sirt2 + Sirt3 | ||
| 7a | <1 | nd | nd |
| 7b | <1 | nd | nd |
| 7c | 3.24 ± 0.27 | 5.21 ± 0.78 | nd |
| 7d | 38.33 ± 0.37 | 19.89 ± 0.89 | 0.77 ± 0.04 |
| 7g | <1 | nd | nd |
| 7h | <1 | nd | nd |
| 13d | 36.34 ± 0.99 | 6.04 ± 0.91 | 0.71 ± 0.03 |
| 13h | 48.54 ± 0.91 | 9.53 ± 0.65 | 0.66 ± 0.02 |
| 13l | 30.06 ± 0.23 | 9.47 ± 0.92 | 0.73 ± 0.06 |
| Ex527 b | 33.33 ± 0.64 | 15.21 ± 0.99 | 0.60 ± 0.02 |
a
The italicized rows show compounds with the highest Sirt1 inhibition. nd = not determined.
b
Biological assay control or standard compound i.e. Ex527.