Table 1.
Inhibitions of AChE, BChE, MAO-A, MAO-B, and BACE-1 by the compounds isolated from C. cuspidataa.
| Compounds | Residual activity at 10 µM (%) | IC50 (µM) | SIb | |||||||
|---|---|---|---|---|---|---|---|---|---|---|
| AChE | BChE | MAO-A | MAO-B | BACE-1 | AChE | BChE | MAO-A | MAO-B | ||
| 1 | 72.5 ± 2.1 | 96.2 ± 3.9 | 91.7 ± 1.6 | 67.2 ± 8.1 | 78.9 ± 0.3 | 37.0 ± 3.0 | > 40 | > 40 | > 40 | > 1.1 |
| 2 | 70.5 ± 5.0 | 90.8 ± 4.2 | 91.3 ± 7.9 | 60.9 ± 5.2 | 91.9 ± 1.0 | 46.4 ± 2.7 | > 40 | > 40 | > 40 | > 0.9 |
| 3 | 55.4 ± 3.4 | 83.3 ± 2.1 | 83.0 ± 6.3 | 43.2 ± 3.7 | 99.7 ± 0.4 | 10.1 ± 0.4 | > 40 | > 40 | 7.27 ± 0.16 | > 4.0 |
| 4 | 53.2 ± 0.0 | 92.3 ± 2.3 | 83.1 ± 4.7 | 89.1 ± 4.1 | 90.1 ± 0.4 | 10.7 ± 1.0 | > 40 | > 40 | > 40 | > 3.7 |
| 5 | 81.5 ± 4.2 | 96.9 ± 5.8 | 99.5 ± 0.7 | 45.4 ± 4.1 | 59.1 ± 0.3 | 41.7 ± 2.4 | > 40 | > 40 | 9.21 ± 0.16 | > 1.0 |
| Toloxatone | 1.08 ± 0.03 | - | ||||||||
| Lazabemide | – | 0.14 ± 0.01 | ||||||||
| Clorgyline | 0.0070 ± 0.0007 | – | ||||||||
| Pargyline | – | 0.030 ± 0.001 | ||||||||
| Tacrine | 0.27 ± 0.02 | 0.060 ± 0.002 | ||||||||
| Donepezil | 0.0095 ± 0.0019 | 0.180 ± 0.004 | ||||||||
aResults shown are the means ± SDs of duplicate or triplicate experiments.
bSI values were calculated by dividing the IC50 for BChE by IC50 for AChE.