F2 values and -fold induction at highest concentration tested (given in parenthesis) for induction of phenacetin O-dealkylase, bupropion hydroxylase, and midazolam 1′-hydroxylase activities in HepaRG cells treated with rifampicin, omeprazole, troglitazone, phenytoin, primaquine, or phenobarbital F2 is the concentration resulting in a 2-fold increase of baseline activities levels. EC50 values are presented when achieved. Values are mean ± S.D. of duplicates in two separate batches of differentiated HepaRG cells.
Phenacetin O-Dealkylase Activity | Bupropion Hydroxylase Activity | Midazolam 1′-Hydroxylase Activity | |||||||
|---|---|---|---|---|---|---|---|---|---|
| F2 | -Fold Induction at Highest Concentration | F2 | -Fold Induction at Highest Concentration | F2 | -Fold Induction at Highest Concentration | ||||
| Rifampicin | N.I.a | N.I. | 0.09 ± 0.04b | 5.9 ± 2.4 (4 μM) | 0.04 ± 0.009 (EC50 = 0.12 ± 0.02b) | 7.9 ± 2.9 (4 μM) | |||
| Omeprazole | 3.2 ± 0.59 | 3.5 ± 1.0 (40 μM) | N.I. | N.I. | N.I. | N.I. | |||
| Troglitazone | N.I. | N.I. | N.I. | N.I. | 0.24 ± 0.10 | 2.2 ± 1.5 (1.56 μM) | |||
| Phenytoin | N.I. | N.I. | 0.41 ± 0.28 | 3.4 ± 2.1 (40 μM) | N.I. | N.I. | |||
| Primaquine | N.I. | N.I. | N.I. | N.I. | N.I. | N.I. | |||
| Phenobarbital | N.I. | N.I. | 7.0 ± 3.8 | 6.2 ± 4.3 (200 μM) | 25 ± 10 | 6.2 ± 2.4 (200 μM) | |||