Characterization of the potency and magnitude of increase in CYP2B6 mRNA and activity by rifampicin, carbamazepine, and estradiol treatment in three cultured human hepatocyte donors
EC50 and Emax values for rifampicin, carbamazepine, and estradiol were determined as described in Materials and Methods.
| Donor | mRNA | |||||
|---|---|---|---|---|---|---|
| Rifampicin | Carbamazepine | Estradiol | ||||
| EC50 (μM) | Emax (fold increase) | EC50mM (μM) | Emax (fold increase) | EC50 (μM) | Emax (fold increase) | |
| mRNA | ||||||
| Hu1399 | 0.45 | 7.7 | 9.4 | 11.5 | 1.7 | 12.7 |
| Hu8127 | 1.4 | 24 | 18 | 15 | 2.5 | 33 |
| Hu4069 | 1.1 | 19 | 51 | 28 | 1.6 | 57 |
| Mean of all donors | 0.98 ± 0.49 | 16.9 ± 8.4 | 26 ± 22 | 18.2 ± 8.7 | 1.9 ± 0.5 | 34 ± 22 |
| Activity | ||||||
| Hu1399 | 0.66 | 4.7 | 74 | 5.6 | 1.6 | 2.2 |
| Hu8127 | 2.0 | 30 | 160 | 33 | 8.8 | 44 |
| Hu4069 | 1.3 | 16 | 202 | 26 | 1.9 | 16 |
| Mean of all donors | 1.3 ± 0.7 | 16.9 ± 12.7 | 145 ± 65 | 21.5 ± 14.3 | 4.1 ± 4.1 | 20 ± 21 |