Table 4.
Compound | ORACa | IC50 ± SDb (μM) |
SIe | IC50 ± SDb (μM) |
SIe | ||
---|---|---|---|---|---|---|---|
ratAChEc | ratBChEd | huAChEf | huBuChEg | ||||
5a | 2.2 ± 0.03 | 6.7 ± 0.31 | 20.9 ± 0.68 | 3.1 | NTh | NTh | – |
5b | 2.1 ± 0.04 | 5.8 ± 0.19 | 17.4 ± 0.52 | 3.0 | NTh | NTh | – |
5c | 2.3 ± 0.02 | 3.9 ± 0.44 | 22.6 ± 0.23 | 5.8 | NTh | NTh | – |
5d | 2.2 ± 0.02 | 2.0 ± 0.46 | 18.1 ± 0.56 | 9.1 | NTh | NTh | – |
5e | 2.5 ± 0.01 | 9.2 ± 0.72 | 13.2 ± 0.43 | 1.4 | NTh | NTh | – |
5f | 2.3 ± 0.03 | 1.7 ± 0.08 | 16.9 ± 0.27 | 9.9 | 0.91 ± 0.02 | 6.3 ± 0.74 | 6.9 |
5g | 2.1 ± 0.02 | 2.5 ± 0.33 | 18.7 ± 0.33 | 7.5 | NTh | NTh | – |
5h | 2.3 ± 0.03 | 3.3 ± 0.09 | 15.5 ± 0.52 | 4.7 | NTh | NTh | – |
5i | 2.1 ± 0.04 | 4.9 ± 0.16 | 14.7 ± 0.62 | 3.0 | NTh | NTh | – |
5j | 2.2 ± 0.05 | 6.5 ± 0.09 | 15.9 ± 0.37 | 2.9 | NTh | NTh | – |
7a | 1.1 ± 0.02 | 10.1 ± 0.41 | 20.2 ± 0.23 | 2.0 | NTh | NTh | – |
7b | 1.2 ± 0.04 | 7.4 ± 0.29 | 18.7 ± 0.37 | 2.5 | NTh | NTh | – |
7c | 1.2 ± 0.02 | 6.7 ± 0.16 | 19.4 ± 0.28 | 2.9 | NTh | NTh | – |
7d | 1.0 ± 0.03 | 9.3 ± 0.37 | 20.3 ± 0.26 | 2.2 | NTh | NTh | – |
7e | 1.5 ± 0.02 | 8.2 ± 0.47 | 15.8 ± 0.62 | 1.9 | NTh | NTh | – |
7f | 1.1 ± 0.03 | 5.4 ± 0.16 | 20.7 ± 0.55 | 3.8 | NTh | NTh | – |
7g | 1.2 ± 0.04 | 1.4 ± 0.08 | 15.7 ± 0.29 | 11.2 | NTh | NTh | – |
7h | 1.0 ± 0.04 | 0.86 ± 0.05 | 16.9 ± 0.34 | 19.7 | NTh | NTh | – |
7i | 1.4 ± 0.03 | 6.1 ± 0.21 | 12.3 ± 0.16 | 2.0 | NTh | NTh | – |
7j | 1.1 ± 0.03 | 1.4 ± 0.08 | 15.7 ± 0.29 | 11.2 | NTh | NTh | – |
7k | 1.2 ± 0.02 | 0.79 ± 0.06 | 14.8 ± 0.36 | 18.7 | 0.57 ± 0.02 | 8.2 ± 0.37 | 14.4 |
7l | 1.2 ± 0.01 | 2.2 ± 0.13 | 15.1 ± 0.28 | 6.9 | NTh | NTh | – |
10a | 1.1 ± 0.01 | 8.1 ± 0.27 | 16.8 ± 0.36 | 2.1 | NTh | NTh | – |
10b | 1.0 ± 0.04 | 4.3 ± 0.38 | 18.6 ± 0.24 | 4.3 | NTh | NTh | – |
10c | 1.2 ± 0.03 | 5.5 ± 0.17 | 13.6 ± 0.67 | 2.5 | NTh | NTh | – |
10d | 1.1 ± 0.02 | 6.4 ± 0.22 | 15.1 ± 0.49 | 2.4 | NTh | NTh | – |
10e | 1.1 ± 0.02 | 7.9 ± 0.26 | 13.8 ± 0.43 | 2.3 | NTh | NTh | – |
10f | 1.0 ± 0.04 | 8.6 ± 0.33 | 16.7 ± 0.52 | 1.9 | NTh | NTh | – |
10g | 1.2 ± 0.03 | 4.6 ± 0.21 | 17.4 ± 0.35 | 3.8 | NTh | NTh | – |
10h | 1.1 ± 0.03 | 0.92 ± 0.06 | 12.9 ± 0.51 | 14.0 | 0.16 ± 0.01 | 3.7 ± 0.06 | 23.1 |
10i | 1.5 ± 0.02 | 6.9 ± 0.14 | 10.3 ± 0.19 | 1.7 | NTh | NTh | – |
10j | 1.2 ± 0.03 | 1.8 ± 0.04 | 15.7 ± 0.24 | 8.7 | NTh | NTh | – |
10k | 1.1 ± 0.02 | 0.81 ± 0.05 | 13.3 ± 0.27 | 16.4 | 0.13 ± 0.01 | 4.5 ± 0.12 | 34.6 |
10l | 1.3 ± 0.03 | 0.62 ± 0.05 | 14.4 ± 0.32 | 23.2 | 0.09 ± 0.002 | 2.2 ± 0.18 | 24.4 |
10m | 1.2 ± 0.02 | 1.3 ± 0.08 | 16.6 ± 0.27 | 12.8 | NTh | NTh | – |
10n | 1.1 ± 0.04 | 3.6 ± 0.11 | 17.9 ± 0.46 | 4.9 | NTh | NTh | – |
10o | 1.2 ± 0.03 | 4.1 ± 0.63 | 16.1 ± 0.25 | 3.9 | NTh | NTh | – |
10p | 1.1 ± 0.02 | 6.2 ± 0.54 | 13.8 ± 0.37 | 2.2 | NTh | NTh | – |
10q | 1.0 ± 0.02 | 4.2 ± 0.15 | 12.2 ± 0.28 | 2.9 | NTh | NTh | – |
10r | 1.2 ± 0.04 | 1.7 ± 0.21 | 14.1 ± 0.22 | 8.3 | NTh | NTh | – |
10s | 1.1 ± 0.03 | 2.6 ± 0.33 | 16.9 ± 0.54 | 6.5 | NTh | NTh | – |
10t | 1.0 ± 0.02 | 5.9 ± 0.37 | 19.3 ± 0.67 | 3.3 | NTh | NTh | – |
10u | 1.2 ± 0.03 | 6.3 ± 0.21 | 17.2 ± 0.45 | 2.7 | NTh | NTh | – |
10v | 1.3 ± 0.03 | 8.1 ± 0.49 | 14.8 ± 0.29 | 1.8 | NTh | NTh | – |
naringenin | 5.2 ± 0.29 | >50 | >50 | – | NTh | NTh | – |
apigenin | 5.6 ± 0.52 | >50 | >50 | – | NTh | NTh | – |
donepezil | NTh | 0.017 ± 0.003 | 16.2 ± 0.31 | 953 | 0.013 ± 0.0004 | 2.7 ± 0.06 | 208 |
aResults are expressed as μM of Trolox equivalent/μM of tested compound. bValues are expressed as the mean ± standard deviation of the mean by 3 independent experiments in triplicate. cFrom 5% rat cortex homogenate. dBuChE from rat serum. eSelectivity Index = IC50 (BuChE)/IC50 (AChE). fFrom human erythrocytes. gFrom human serum. hNT = not tested.