Table 3.
In vitro inhibition of soybean lipoxygenase (IC50 μM or LOX Inh. %) and in vitro inhibition of acetyl-cholinesterase (IC50 μM or AChE Inh. %); experimentally-determined lipophilicity RM; theoretically calculated lipophilicity values cLogP.
| Compound | % LOX Inhb. @ 100 μM/IC50 μM | % AChE Inhb. @ 100 μM/IC50 μM | RM ± (SD) ¥ | cLogP |
|---|---|---|---|---|
| a1 * | 14 | 7 | 0.34 | 5.51 |
| a2 * | 10 | 26 | 0.36 | 5.06 |
| a3 * | 56/100 μM | 50/100 μM | −0.69 | 3.58 |
| a4 * | 44 | 25 | −0.26 | 4.13 |
| a5 | 9 | 38 | −0.62 | 2.60 |
| a6 | 60 | Νο | −0.65 | 1.91 |
| a7 | 4 | 63/87 μM | −0.64 | 3.41 |
| a8 | 14 | 57/100 μM | −0.68 | 3.81 |
| a9 | 16 | 48 | −0.82 | 3.90 |
| a10 | 23 | 27 | −0.06 | 2.13 |
| a11 | 36 | 56/100 μM | −1.09 | 3.15 |
| a12 | 2 | 42 | −0.81 | 2.63 |
| a13 | 23 | 25 | −0.73 | 2.96 |
| b1 | 89/56 μM | 89/100 μM | −0.91 | 5.97 |
| b2 | 44 | 44 | 0.04 | 5.52 |
| b3 | 100/57 μM | 100 # | −0.66 | 4.04 |
| b4 | 82/65 μM | 82 # | −0.03 | 4.59 |
| b7 | 29 | 29 | −0.85 | 3.87 |
| b8 | 25 | 25 | −0.79 | 4.27 |
| b9 | 16 | 16 | −0.37 | 4.36 |
| b11 | 31 | 31 | −0.91 | 3.61 |
| b13 | 14 | 14 | 0.43 | 3.42 |
| di | 12 | 22 | 0.67 | 3.31 |
| Dii * | no | 20 | −0.23 | 3.68 |
| diii | 41 | 29 | −0.37 | 3.97 |
| div | 17 | 29 | 0.23 | 4.49 |
| dv | 7 | 18 | −0.53 | 5.02 |
| dvi | 17 | 12 | 0.32 | 5.59 |
| dvii | 5 | 27 | −0.36 | 6.08 |
| c1 * | 41 | 23 | −0.68 | 10.88 |
| c2 * | 100/55 μM | 71/49 μM | −0.89 | 7.92 |
| c3 * | 93/56 μM | 95/52 μM | 0.77 | 9.03 |
| c4 * | 100/55 μM | 58/100 μM | 0.43 | 5.98 |
| c5 | 32 | 51/100 μM | 0.43 | 5.98 |
| c6 | 98/54 μM | Νο | −0.97 | 5.54 |
| c7 | 41 | 94/56 μM | −0.77 | 7.59 |
| c8 | 26.5 | 100/58 μM | −0.85 | 8.39 |
| c9 | 24.5 | 85/74 μM | −0.86 | 8.58 |
| c10 | 57/85 μM | 69/76 μM | 0.7 | 5.04 |
| c11 | 95/50 μM | 100/52 μM | −0.88 | 7.08 |
| c12 | 52/96 μM | 100/48 μM | −0.96 | 6.04 |
| c13 | 76/65 μM | 50.5/100 μM | 0.34 | 6.69 |
| ei | 77/62.5 μM | 71/57.5 μM | 0.56 | 7.55 |
| eiii | 27 | 47 | −0.07 | 8.21 |
| eiv | 23 | 72/76 μM | 0.13 | 8.74 |
| ev | 7 | 14 | Nd | 9.27 |
| evi | 65/76 μM | 64/62 μM | Nd | 9.79 |
| evii | 12 | 6/85 μM | Nd | 10.4 |
| Tacrine | 98/0.03 μM | |||
| NDGA | 93/0.5 μM |
* [29] # % activity at 0.001 µM; ¥ SD < 10%; Means within each column differ significantly (p < 0.05); nd: not determined under the experimental conditions.