Table 1. Summary of the impact of prototypical inducers (Chenodeoxycholiic acid; CDCA, Pregnane 16α-carbonitrile; PCN, Phenobarbital; PB and Rifampicin; RIF), on gene expression in H411e, Iec-6, and rat primary hepatocytes. For clarity, statistical analyses for cell lines H411e and Iec-6 are given only for the lowest concentration at which a significant difference was observed. For primary hepatocytes, the incubation time (in hours) when significant induction was detected: bP<0.05, cP<0.01.
H411e Test compound (μmol/L) | Iec-6 Test compound (μmol/L) | Primary hepatocytes Test compound at 1 μmol/L (Incubation time in hours) | ||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|
Gene | CDCA | PCN | PB | RIF | CDCA | PCN | PB | RIF | CDCA | PCN | PB | RIF |
CYP2B2 | 0.1c | 0.1c | 10b | NS | 1c | 0.1c | NS | NS | 2c | 2c | 2b | NS |
CYP3A1 | 10b | 0.1c | 10b | 1c | 0.1c | 0.01c | 1c | 0.1b | 2c | 2b | 2c | 2c |
CYP3A2 | NS | 0.1c | 10b | 1c | NS | 10c | 1b | 1c | 2c | 2c | 2c | 2c |
CYP3A9 | 0.1c | 0.1c | 10c | 0.01b | NS | 0.01c | 0.01c | 0.1c | 2c | 2c | 2c | 2c |
ABCC1 | 1c | 1c | NS | 1c | 1c | 1c | NS | 1b | 4b | 2c | 2b | 4b |
ABCC2 | 1b | 1c | 10c | 1c | NS | NS | 1b | 1c | 2c | 2b | 2b | 2b |
ABCB1a | 0.01c | 0.01c | 0.01c | 0.01c | 0.01c | 0.01c | 0.01c | 0.01c | 2b | 2c | 2c | 4c |
ABCB1b | 0.1c | 0.01c | 0.01c | 0.1c | 1c | 0.01c | 0.01c | 0.1c | 2c | 2b | 2c | 2c |
FXR | 1c | 0.1c | NS | 1c | 0.1b | NS | NS | NS | 2c | NS | NS | NS |
PXR | 10b | NS | 0.1c | 1c | 1b | 0.1b | 0.1b | 0.1c | NS | 2b | 2c | 2c |
CAR | 1c | 1c | 10c | 1c | 1c | 0.1b | 0.1c | 0.1c | 2b | 4b | 2c | 2c |