P450 fold-induction in drug-induced human hepatocyte cultures compared to DMSO-treated cells
Values are the average P450 mRNA induction ratios in response to 48-h treatment of 2.5 μM 3-MC, 50 μM RIF, 50 μM DEXA, and 2 mM PB in human hepatocyte cultures. The fold-induction is compared to DMSO-treated cells.
P450 | 3-MC | RIF | DEXA | PB |
|---|---|---|---|---|
| CYP1A1 | 441.9 ± 360.6* | 5.1 ± 1.8* | 1.5 ± 0.2* | 0.9 ± 0.2 |
| CYP1A2 | 107.6 ± 179.6* | 1.7 ± 1.3 | 1.1 ± 0.2 | 0.4 ± 0.1* |
| CYP1B1 | 46.8 ± 90.0* | 1.4 ± 0.2 | 0.9 ± 0.1 | 1.1 ± 0.4 |
| CYP2A6 | 0.8 ± 0.2 | 4.6 ± 5.1 | 1.8 ± 1.0 | 4.1 ± 2.6* |
| CYP2A7 | 0.8 ± 0.3 | 3.6 ± 3.5 | 1.9 ± 0.8 | 6.7 ± 3.7 |
| CYP2A13 | 1.0 ± 0.3 | 1.2 ± 0.8 | 1.1 ± 0.6 | 1.4 ± 0.5 |
| CYP2B6 | 1.2 ± 0.2 | 9.7 ± 5.2* | 3.4 ± 1.4* | 8.6 ± 3.3* |
| CYP2C8 | 0.9 ± 0.1 | 3.6 ± 1.5 | 2.0 ± 1.4 | 1.4 ± 0.7 |
| CYP2C9 | 0.9 ± 0.1 | 1.8 ± 0.6 | 1.3 ± 0.5 | 0.9 ± 0.1 |
| CYP2C18 | 1.0 ± 0.1 | 0.5 ± 0.1 | 0.8 ± 0.1 | 0.7 ± 0.1 |
| CYP2C19 | 0.9 ± 0.1 | 3.3 ± 1.4 | 1.1 ± 0.3 | 1.3 ± 0.2 |
| CYP2D6 | 1.0 ± 0.2 | 1.4 ± 0.5 | 1.2 ± 0.3 | 1.0 ± 0.4 |
| CYP2E1 | 0.8 ± 0.3 | 0.3 ± 0.2* | 0.6 ± 0.3 | 0.1 ± 0.1* |
| CYP2F1 | N.D. | N.D. | N.D. | N.D. |
| CYP2J2 | 1.0 ± 0.2 | 0.8 ± 0.1 | 1.0 ± 0.1 | 0.5 ± 0.1 |
| CYP2R1 | 1.0 ± 0.1 | 0.7 ± 0.2 | 0.9 ± 0.1 | 1.0 ± 0.2 |
| CYP2S1 | 1.8 ± 1.2 | 1.4 ± 0.6 | 0.8 ± 0.5 | 1.2 ± 0.4 |
| CYP2U1 | 0.9 ± 0.1 | 1.0 ± 0.2 | 1.1 ± 0.2 | 0.8 ± 0.2 |
| CYP2W1 | N.D. | N.D. | N.D. | N.D. |
| CYP3A4 | 0.8 ± 0.2 | 15.5 ± 22.5* | 2.8 ± 1.5* | 2.1 ± 0.8* |
| CYP3A5 | 0.9 ± 0.1 | 1.2 ± 0.3 | 1.0 ± 0.2 | 1.0 ± 0.2 |
| CYP3A7 | 1.0 ± 0.2 | 1.6 ± 1.4 | 1.6 ± 0.4 | 0.7 ± 0.2 |
| CYP3A43 | 0.8 ± 0.2 | 3.9 ± 2.7 | 1.1 ± 0.4 | 0.9 ± 0.1 |
N.D., not determined.
↵* Significantly different from 1.0 (level in corresponding control cells), P < 0.05, using the distribution-free Wilcoxon paired t test.