Table 1. Effect of the ethanolic extract of Antrodia cinnamomea (EEAC) on rhodamine123 transport by wild-type and variant-type human P-gp.
Nonlinear kinetic parameters | |||
ABCB1 1236C-2677G-3435C (wild-type) | Vm (pmole/mg protein/10 mins) | Km (µM) | |
Nonlinear regression | |||
Rhodamine 123 only | 11.22±0.73 | 20.17±4.45 | |
+ EEAC, 1 µg/ml | 5.12±0.73* | 21.9±3.26 | |
+ EEAC, 5 µg/ml | 3.95±1.03* | 20.44±6.28 | |
EEAC Ki estimation | |||
Ki from Lineweaver–Burk (µg/ml) | 4.5±0.83 | ||
IC50 (µg/ml) | 1.51±0.08 | ||
ABCB1 1236T-2677T-3435T | |||
Nonlinear regression | |||
Rhodamine 123 only | 9.84±1.16 | 24.54±1.94 | |
+ EEAC, 1 µg/ml | 4.49±0.66* | 19.24±5.11 | |
+ EEAC, 5 µg/ml | 3.65±0.18* | 16.83±3.23 | |
EEAC Ki estimation | |||
Ki from Lineweaver–Burk (µg/ml) | 6.32±1.18 | ||
IC50 (µg/ml) | 5.56±0.49 | ||
ABCB1 1236T-2677A-3435T | |||
Nonlinear regression | |||
Rhodamine 123 only | 3.54±0.18 | 23.8±0.5 | |
+ EEAC, 1 µg/ml | 1.54±0.1* | 10.7±2.91* | |
+ EEAC, 5 µg/ml | 0.89±0.16* | 8.65±1.35* | |
EEAC Ki estimation | |||
Ki from Lineweaver–Burk (µg/ml) | 1.45±0.66 | ||
IC50 (µg/ml) | 3.33±0.67 |
*p<0.05 compared with rhodamine123 transport without EEAC.