Effect of E-sul on the uptake of tel-glu and E217βG by cryopreserved human hepatocytes in the presence of 0.3% HSA
The substrate concentration used was 2 and 50 μM for tel-glu and 1 and 200 μM for E217βG. The saturable uptake of tel-glu and E217βG into cyropreserved human hepatocytes was determined after the subtraction of nonsaturable uptake (evaluated as the uptake clearance in the presence of 50 μM tel-glu or 200 μM E217βG). The term “% control” represents the ratio of the uptake clearance in the presence of 30 μM E-sul to that in its absence.
| HH-OCF | HH-094 | HH-TDH | ||||
|---|---|---|---|---|---|---|
| E217βG | Tel-Glu | E217βG | Tel-Glu | E217βG | Tel-Glu | |
| μl/min/106 cells | ||||||
| E-sul | ||||||
| 0 μM | 5.66 ± 1.05a | 12.8 ± 0.7 | 1.85 ± 0.72a | 15.7 ± 0.7 | 2.08 ± 0.5 | 11.4 ± 2.5 |
| 30 μM | 1.50 ± 0.75a | 9.84 | 1.03 ± 0.76a | 14.1 ± 1.0 | 0.0472 ± 0.1155 | 10.6 ± 0.4 |
| % control | 26.6% | 76.9% | 55.8% | 89.9% | 2.3% | 93.0% |
↵ a Values from Ishiguro et al. (2006).