Effects of furanocoumarins on the permeability of digoxin
Papp, AB and Papp, BA values show the apparent permeability of digoxin through the Caco-2 monolayer from the apical-to-basal and basal-to-apical direction, respectively. Initial concentrations of both digoxin and furanocoumarins were adjusted to 10 μM. The initial concentration of cyclosporine A (positive control) was adjusted to 20 μM. The efflux ratio was calculated from eq. 4. Each value represents the mean ± S.E. (n = 3).
| Position | Addition | Papp, AB | Papp, BA | Efflux Ratio | |
|---|---|---|---|---|---|
| ×10−5 cm/s | |||||
| Control | 10 μM Digoxin | 0.66 ± 0.05 | 19.20 ± 1.26 | 29.20 | |
| Positive control +10 μM Furanocoumarin | +20 μM Cyclosporine A | 5.21 ± 0.47 | 5.50 ± 1.18 | 1.06** | |
| Side chain | 5 | +Notopterol | 0.96 ± 0.08 | 17.80 ± 1.71 | 18.50 |
| 5 and 8 | +Byakangelicol | 1.77 ± 0.16 | 14.10 ± 1.32 | 7.97** | |
| Dimer | +Rivulobirin A | 2.88 ± 0.31 | 10.70 ± 2.12 | 3.72** | |
↵** Significant at p < 0.01 vs. control.