Table 1.
Inhibitory activities on human AChE and BuChE, BACE1, Aβ1-42 self-aggregation, Aβ1-42 oligomer cytotoxicity of the studied compounds.
| Compounds | IC50 μmol/L ± SEM1 | |||||
|---|---|---|---|---|---|---|
| hAChE | hBuChE | BACE1 | Aβ1-42 self-aggregation | Aβ1-42 oligomer toxicity | ||
| SH-SY5Y cells | THP-1 cells | |||||
| AP2238 | 0.044 ± 0.0062 | 48.9 ± 3.72 | − | ≫503 | – | – |
| AP2243 | 0.018 ± 0.0034 | 118 ± 163 | 0.24 ± 0.03 | ≫503 | ≫303 | ≫303 |
| AP2469 | 8.60 ± 0.21 | 124 ± 13 | 6.49 ± 0.31 | 21.7 ± 3.4 | 7.50 ± 0.72 | 8.18 ± 0.51 |
| Galantamine | 2.01 ± 0.15 | 20.7 ± 1.5 | >53,5 | ≫503 | 7.99 ± 0.91 | ≫303 |
1
Concentration of compound resulting in 50% inhibition of human AChE, BuChE, BACE1 activity, Aβ1-42 self-aggregation, and Aβ1-42 oligomer cytotoxicity.
2
From Piazzi et al. 2003.
3
Not active at the highest tested concentration (50 μmol/L, 30 μmol/L or 5 μmol/L).
4
From Piazzi et al. 2007.
5
From Mancini et al. 2007.