Table 2. Inhibitory Activitiesa (μM) of the Investigated Compounds 1–14 against Aβ Aggregation, ChEs, and MAOs.
IC50 (μM) or (% inhibition)b |
|||||
---|---|---|---|---|---|
compd | Aβ40 aggr | eeAChE | esBChE | hMAO A | hMAO B |
1 | (63 ± 3)c | (39 ± 1) | (8 ± 3) | (<5) | (22 ± 4) |
2 | 3.2 ± 0.8 | 9.2 ± 0.6 | (26 ± 3) | 3.6 ± 0.3 | 0.0077 ± 0.0013 |
3 | 4.4 ± 0.3 | 7.9 ± 0.8 | (24 ± 1) | (41 ± 3) | 0.031 ± 0.001 |
4 | 8.2 ± 0.3 | 3.5 ± 0.3 | (35 ± 3) | 3.0 ± 0.2 | 0.054 ± 0.001 |
5 | 6.6 ± 0.1 | 8.7 ± 0.8 | (29 ± 4) | 5.0 ± 0.2 | 0.11 ± 0.01 |
6 | 19 ± 4 | 6.8 ± 0.7 | (24 ± 4) | (23 ± 4) | (24 ± 6) |
7 | 8.7 ± 0.4 | 1.7 ± 0.1 | (15 ± 3) | (21 ± 6) | 0.48 ± 0.08 |
8 | 17 ± 2 | 13 ± 2 | (14 ± 3) | (26 ± 6) | 2.7 ± 0.8 |
9 | 14 ± 2 | 11 ± 1 | (17 ± 1) | (22 ± 2) | (52 ± 3) |
10 | (62 ± 2)c | 8.7 ± 0.5 | (24 ± 3) | 1.1 ± 0.3 | (34 ± 3) |
11 | 2.1 ± 0.2 | 7.3 ± 0.7 | 1.7 ± 0.3 | 3.1 ± 0.3 | 0.57 ± 0.02 |
12 | 1.9 ± 0.3 | 7.84 ± 0.03 | 8.2 ± 0.4 | (50 ± 3) | 0.24 ± 0.05 |
13 | (57 ± 5)c | 1.85 ± 0.04 | (17 ± 1) | (25 ± 5) | (42 ± 1) |
14 | 11 ± 2 | 8.1 ± 0.5 | 3.4 ± 0.2 | (53 ± 3) | 0.98 ± 0.14 |
quercetin | 0.82 ± 0.07 | ||||
donepezil | 0.021 ± 0.002 | 2.3 ± 0.1 | |||
safinamide | (18 ± 3) | 0.031 ± 0.001 |
Data are the mean ± SEM of n = 3 experiments.
Data in parentheses correspond to % of inhibition at 10 μM, or
100 μM for inhibition of Aβ40 aggregation.