Table 2.
Compound | %Inhibition hAChE ± SD a |
hAChE IC50 ± SD (µM) b | % inhibition hBuChE ± SD a |
hBuChE IC50 ± SD (µM) b | SI for hBuChE c |
POP IC50 ± SD (µM) b |
---|---|---|---|---|---|---|
Lycosinine B (1) | 28 ± 1 | >100 | 42 ± 1 | >100 | nc | 258 ± 14 |
Trispheridine (2) | 6 ± 1 | >100 | 13 ± 1 | >100 | nc | nm |
3,4-Anhydrogalanthamine (3) | 4 ± 0 | >100 | 28 ± 1 | >100 | nc | nm |
Carltonine A (13) | 2 ± 0 | >100 | 98 ± 1 | 0.91 ± 0.02 | >110 | 143 ± 12 |
Carltonine B (14) | 40 ± 1 | >100 | 99 ± 1 | 0.031 ± 0.001 | >3226 | nm |
Carltonine C (15) | 9 ± 0 | >100 | 78 ± 1 | 14.8 ± 1.1 | >7 | nm |
Galanthamine d | nm | 1.72 ± 0.12 | nm | 42 ± 1 | 0.04 | nm |
Eserine d | nm | 0.063 ± 0.005 | nm | 0.13 ± 0.01 | 0.48 | nm |
Berberine d | nm | 0.72 ± 0.11 | nm | 31 ± 4 | 0.02 | 142 ± 21 |
a Tested at 100 µM compound concentration; b Compound concentration required to decrease enzyme activity by 50%; the values are the mean values ± standard deviations (SD) of three independent measurements, each performed in triplicate; c Selectivity index (SI) for hBuChE is determined as ratio hAChE IC50/hBuChE IC50; d Reference compound; nc stands for not calculated; nm stands for not measured.