Table 2. Enzyme Inhibition Activities of Compounds 1–26a.
|
anticholinesterase
activity |
||||||
|---|---|---|---|---|---|---|
| compound | AChE IC50(μM) | BChE IC50(μM) | SI for AChEb | SI for BChEb | tyrosinase activity IC50(mM) | urease activity IC50(μM) |
| 1 | 129.95 ± 0.18 | 118.46 ± 0.34 | 0.91 | 1.10 | 35.13 ± 0.07 | 82.54 ± 0.29 |
| 2 | 44.30 ± 0.75 | 66.44 ± 0.41 | 1.50 | 0.67 | 30.25 ± 0.61 | 65.43 ± 0.67 |
| 3 | 34.22 ± 0.63 | 48.72 ± 0.18 | 1.42 | 0.70 | 29.44 ± 0.49 | 56.80 ± 0.15 |
| 4 | 27.65 ± 0.51 | 39.60 ± 0.74 | 1.43 | 0.70 | 28.41 ± 0.90 | 56.11 ± 0.22 |
| 5 | 26.99 ± 0.48 | 37.11 ± 0.57 | 1.38 | 0.73 | 28.04 ± 0.35 | 55.64 ± 0.81 |
| 6 | 28.95 ± 0.64 | 36.81 ± 0.19 | 1.27 | 0.79 | 27.99 ± 0.17 | 50.78 ± 0.08 |
| 7 | 30.45 ± 0.47 | 40.88 ± 0.16 | 1.34 | 0.75 | 27.72 ± 0.24 | 54.34 ± 0.62 |
| 8 | 33.61 ± 0.33 | 47.27 ± 0.77 | 1.41 | 0.71 | 25.68 ± 0.39 | 53.37 ± 0.64 |
| 9 | 29.80 ± 0.81 | 40.19 ± 0.19 | 1.35 | 0.74 | 25.42 ± 0.12 | 51.70 ± 0.12 |
| 10 | 26.48 ± 0.25 | 37.53 ± 0.20 | 1.42 | 0.71 | 25.00 ± 0.67 | 49.28 ± 0.55 |
| 11 | 21.45 ± 0.06 | 32.77 ± 0.48 | 1.53 | 0.66 | 23.41 ± 0.50 | 31.52 ± 0.49 |
| 12 | 17.41 ± 0.22 | 24.43 ± 0.51 | 1.40 | 0.71 | 24.78 ± 0.77 | 23.60 ± 0.70 |
| 13 | 20.05 ± 0.37 | 32.21 ± 0.11 | 1.61 | 0.62 | 26.16 ± 1.11 | 30.28 ± 0.95 |
| 14 | 19.21 ± 0.61 | 25.72 ± 1.05 | 1.34 | 0.75 | 8.10 ± 0.22 | 26.70 ± 0.52 |
| 15 | 27.40 ± 0.76 | 37.63 ± 0.61 | 1.37 | 0.73 | 5.19 ± 0.03 | 46.37 ± 1.08 |
| 16 | 29.04 ± 1.03 | 42.50 ± 0.18 | 1.46 | 0.69 | 24.08 ± 0.15 | 42.03 ± 0.81 |
| 17 | 34.76 ± 0.53 | 49.80 ± 1.01 | 1.43 | 0.70 | 3.22 ± 0.70 | 40.22 ± 0.12 |
| 18 | 21.44 ± 0.92 | 32.90 ± 0.75 | 1.54 | 0.65 | 16.04 ± 0.41 | 20.24 ± 0.77 |
| 19 | 20.59 ± 0.55 | 29.73 ± 0.72 | 1.44 | 0.69 | 19.28 ± 0.09 | 18.25 ± 0.50 |
| 20 | 26.84 ± 0.77 | 34.05 ± 0.06 | 1.26 | 0.79 | 21.45 ± 0.31 | 16.79 ± 0.19 |
| 21 | 20.65 ± 1.02 | 28.14 ± 0.55 | 1.36 | 0.73 | 11.16 ± 0.39 | 27.82 ± 0.51 |
| 22 | 24.78 ± 0.30 | 33.01 ± 0.84 | 1.33 | 0.75 | 9.13 ± 0.55 | 26.16 ± 0.47 |
| 23 | 19.73 ± 0.54 | 25.42 ± 0.26 | 1.29 | 0.78 | 8.05 ± 0.11 | 24.97 ± 0.54 |
| 24 | 19.52 ± 0.29 | 25.66 ± 0.69 | 1.32 | 0.76 | 7.21 ± 0.27 | 22.49 ± 0.11 |
| 25 | 19.80 ± 0.50 | 25.46 ± 0.78 | 1.29 | 0.78 | 8.40 ± 0.64 | 21.70 ± 0.06 |
| 26 | 19.84 ± 0.37 | 25.70 ± 0.53 | 1.30 | 0.77 | 8.76 ± 0.90 | 21.51 ± 0.44 |
| galantaminec | 4.48 ± 0.78 | 46.03 ± 0.14 | 10.28 | 0.10 | NT | NT |
| kojic acidc | NT | NT | 0.66 ± 0.42 | NT | ||
| IQl-mimosinec | NT | NT | 0.70 ± 0.11 | NT | ||
| thioureac | NT | NT | NT | 24.20 ± 0.3 | ||
Values expressed are the mean ± SEM of three parallel measurements (p < 0.05).
Selectivity index for AChE: IC50 for BChE/IC50 for AChE. Selectivity index for BChE: IC50 for AChE/IC50 for BChE. NT: not tested.
Reference compounds.