Table 1.
In vitro α-glucosidase inhibitory activity of honokiol thioethers.a
| Compound | Substituent (R) | Inhibition rate (%) | IC50 (µM) |
|---|---|---|---|
| 7a | –Ph | 6.3 ± 1.7 | –b |
| 7b | –(2-F)Ph | 33.9 ± 2.8 | – |
| 7c | –(3-F)Ph | 14.6 ± 1.9 | – |
| 7d | –(4-F)Ph | 8.4 ± 0.4 | – |
| 7e | –(2-Cl)Ph | 19.4 ± 3.1 | – |
| 7f | –(3-Cl)Ph | 10.4 ± 1.4 | – |
| 7g | –(4-Cl)Ph | 57.9 ± 2.6 | – |
| 7h | –(2-Br)Ph | 91.5 ± 0.1 | 25.8 ± 2.3 |
| 7i | –(3-Br)Ph | 12.4 ± 2.3 | – |
| 7j | –(4-Br)Ph | 22.4 ± 1.4 | – |
| 7k | –(2-CH3)Ph | 95.3 ± 1.6 | 25.0 ± 1.9 |
| 7l | –(3-CH3)Ph | 95.2 ± 0.4 | 18.9 ± 2.3 |
| 7m | –(4-CH3)Ph | 13.5 ± 0.3 | – |
| 7n | –(2-OCH3)Ph | 25.2 ± 1.6 | – |
| 7o | –(3-OCH3)Ph | 95.5 ± 0.7 | 24.5 ± 2.0 |
| 7p | –(4-OCH3)Ph | 9.9 ± 0.4 | – |
| 9a | -Ph | 69.8 ± 3.8 | – |
| 9c | –(3-F)Ph | 53.5 ± 1.5 | – |
| 9e | –(2-Cl)Ph | 64.5 ± 2.5 | – |
| 9g | –(4-Cl)Ph | 7.1 ± 1.3 | – |
| 9j | –(4-Br)Ph | 3.7 ± 0.1 | – |
| 9k | –(2-CH3)Ph | 64.5 ± 2.1 | – |
| 9l | –(3-CH3)Ph | 78.2 ± 0.1 | – |
| 9m | –(4-CH3)Ph | 6.7 ± 0.6 | – |
| 9o | –(3-OCH3)Ph | 81.8 ± 2.1 | 52.9 ± 3.4 |
| 9q | –(4-NO2)Ph | 79.5 ± 0.1 | – |
| 9r | 3-pyridyl | 33.2 ± 2.1 | – |
| honokiol | / | 17.1 ± 1.7 | – |
| acarbosec | / | 96.4 ± 0.5 | 24.4 ± 0.3 |
a
Values are expressed as mean ± SD (n = 3).
b
Not determined; cAcarbose was used as the positive control.