CYP2B6 induction in primary human hepatocytes
Human hepatocytes from five donors cultured in six-well Biocoat plates were treated for 24 h with DMSO (0.1%), 10 μM RIF, 1 μM CITCO, and the indicated concentrations of CMZ, EFV, and NVP. Total RNA was extracted from one to two wells per treatment, reverse-transcribed, and subjected to TaqMan real-time PCR. CYP2B6 mRNA levels were normalized to those of β-actin. Fold induction data relative to vehicle control represent the mean of triplicate PCR determinations.
Drug | Hu177 | Hu190 | Hu214 | HCS009 | HCS014 |
|---|---|---|---|---|---|
| CMZ | |||||
| 1 | NA | 1.6 | 1.3 | 2.0 | 1.4 |
| 10 | 6.0 | 4.3 | 4.6 | 4.9 | 2.9 |
| 25/50a | 10.5 | 8.6 | 4.9 | 6.5 | 4.1 |
| EFV | |||||
| 1 | 4.4 | 3.4 | 2.1 | 4.2 | 1.9 |
| 5/10b | 7.9 | 7.9 | 2.8 | 6.2 | 2.6 |
| 10/25b | 5.5 | 7.4 | 3.3 | 5.8 | 3.7 |
| NVP | |||||
| 1 | 1.4 | 1.6 | 1.3 | 1.6 | 1.0 |
| 10 | 3.4 | 4.1 | 3.9 | 4.5 | 1.8 |
| 50 | 6.2 | 12.0 | 8.2 | 9.8 | 3.7 |
| RIF | |||||
| 10 | NA | 9.7 | 10.8 | 4.5 | 3.2 |
| CITCO | |||||
| 1 | 13.0 | 25.8 | NA | 10.8 | 5.3 |