Characterization of noninduced Caco-2 as well as vinblastine-induced and MDR-1-transfected Caco-2 cells with respect to expression of P-gp
| Compound | Donor Concentration | Fluxrates | Mean Factor of Increase | |||||
|---|---|---|---|---|---|---|---|---|
| Noninduced Caco-2 | Vinblastine-induced Caco-2 | |||||||
| a → b | b → a | Secretory | a → b | b → a | Secretory | |||
| μm | pmol/cm2/h | |||||||
| Vinblastine | 0.1 | 0.15 ± 0.03 | 6.2 ± 0.7 | 6.0 ± 0.7 | 0.09 ± 0.005 | 10.5 ± 0.3 | 10.4 ± 0.03 | 1.7 |
| R-Talinolol | 250 | 201 ± 61 | 1219 ± 111 | 1013 ± 172 | 146 ± 67 | 1788 ± 192 | 1642 ± 259 | 1.6 |
| S-Talinolol | 250 | 189 ± 65 | 1199 ± 113 | 920 ± 178 | 134 ± 66 | 1718 ± 168 | 1584 ± 234 | 1.7 |
| Quinidine | 0.25 | 20.0 ± 0.4 | 47.0 ± 0.8 | 27.0 ± 1.2 | 9.0 ± 0.4 | 74.8 ± 8.0 | 65.8 ± 8.4 | 2.4 |
| MDR-1 transfected Caco-2 | ||||||||
| a → b | b → a | Secretory | ||||||
| R-Talinolol | 250 | 23.0 ± 8.9 | 1282 ± 73 | 1259 ± 84 | 1.2 | |||
| S-Talinolol | 250 | 18.1 ± 8.4 | 1253 ± 60 | 1234 ± 68 | 1.3 | |||
| Quinidine | 0.25 | 3.5 ± 0.3 | 42 ± 2.5 | 38.5 ± 2.8 | 1.4 | |||
Typical results for net secretory flux as determined by transport experiments using monolayers of the respective cell line (mean ± S.D., n = 3 for each compound and direction), as well as the resulting mean increase in secretory flux.