Cholinesterase inhibitory activity and extracellular APP and cell viability as a percentage of control values
sAPP ELISA | Viability MTT | Ratio APP/MTT | IC50 AChE | IC50 BChE | clog Pa | ||
|---|---|---|---|---|---|---|---|
| 20 μM | nM ± S.E.M. | ||||||
| A | 35 | 94 | 0.37 | >10,000 | 2600 ± 135 | 1.51 | |
| B | 38 | 65 | 0.58 | 110 ± 9 | 40 ± 9 | 3.96 | |
| C | 63 | 99 | 0.64 | >10,000 | 9 ± 1.3 | 6.02 | |
| D | 75 | 94 | 0.80 | >10,000 | >10,000 | 6.19 | |
| E | 29 | 50 | 0.58 | >10,000 | 3 ± 0.5 | 4.56 | |
| F | 88 | 94 | 0.94 | >10,000 | >10,000 | 1.54 | |
| G | 68 | 84 | 0.72 | 650 ± 95 | 1100 ± 175 | 3.10 | |
| H | 84 | 99 | 0.85 | >10,000 | 4 ± 0.2 | 5.72 | |
↵ a clog P value is a calculated assessment of lipophilicity (log octanol/water partition coefficient) determined at pH 7.0. (Pallas; CompuDrug International, Sedona, AZ). A value of log 1.0 and greater is commensurate with a rapid blood-brain barrier penetrability. There was no significant correlation between either AChE or BChE IC50 values and percentage of inhibition of sAPP or cell viability (p > 0.05 for all coefficients of linear regression analyses)