Table 2. HZ08 inhibition of VER-stimulated P-gp ATPase activity.
ATP | Fold stimulation | |
---|---|---|
pmol ATP consumed/ μg P-gp / min | ||
Non-treated | 17.18±7.14 | / |
VER(100μM) | 78.04±1.38 | 4.54 |
+ HZ08 (0.625μM) | 74.09±4.02 | 4.31 |
+ HZ08 (1.25μM) | 73.10±1.34* | 4.26 |
+ HZ08 (2.5μM) | 69.42±1.31** | 4.04 |
+ HZ08 (5μM) | 66.82±0.87*** | 3.89 |
+ HZ08 (10μM) | 63.11±1.71*** | 3.67 |
+ HZ08 (20μM) | 55.21±0.43*** | 3.21 |
+ HZ08 (40μM) | 41.25±3.00*** | 2.40 |
+ HZ08 (80μM) | 34.48±1.56*** | 2.01 |
Data are presented as mean±SD, n = 3
*P<0.05
**P<0.01
***P< 0.001 compared to the value from VER single agent treatment wells.