Table 2.
Induction of different cytochrome P450 isoenzymes in cultured human hepatocytes from five different donors with Helixor® A (HA), Helixor® M (HM) and Helixor® P (HP). Fold induction of activity over respective negative control (incubation with no test item) is given. Test mixtures containing reference inducers were used as positive controls (PC)
| CYP | CYP1A2 | CYP2B6 | CYP2C9 | CYP2E1 | CYP3A4 | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Donor | D1 | D2 | D3 | D1 | D4 | D5 | D1 | D4 | D5 | D1 | D2 | D3 | D1 | D2 | D3 |
| PC | 19.2 | 21.8 | 31.6 | 3.0 | 3.7 | 2.9 | 1.5 | 1.3 | 1.5 | 1.2 | 1.0 | 1.0 | 1.7 | 1.9 | 3.3 |
| HA 10 μg/ml | 0.5 | 0.8 | 0.4 | 1.0 | 0.6 | 1.2 | 0.6 | 0.6 | 0.4 | 0.9 | 0.6 | 0.8 | 1.0 | 0.7 | 0.9 |
| HA 5 μg/ml | 0.6 | 1.1 | 0.4 | 1.0 | 0.9 | 1.2 | 0.6 | 1.1 | 1.0 | 1.0 | 0.6 | 1.0 | 1.4 | 0.8 | 0.9 |
| HA 0.5 μg/ml | 0.8 | 1.2 | 0.4 | 1.0 | 1.1 | 0.8 | 0.9 | 1.2 | 0.4 | 0.9 | 0.7 | 1.0 | 1.4 | 0.9 | 1.1 |
| HM 10 μg/ml | 0.6 | 0.8 | 0.3 | 0.6 | 0.2 | 0.9 | 0.5 | 0.1 | 0.8 | 0.9 | 0.7 | 0.8 | 0.7 | 0.4 | 0.4 |
| HM 5 μg/ml | 0.6 | 1.0 | 0.4 | 1.2 | 0.8 | 1.2 | 0.8 | 0.7 | 0.9 | 1.1 | 0.9 | 1.3 | 1.1 | 0.5 | 0.9 |
| HM 0.5 μg/ml | 0.8 | 1.1 | 0.4 | 1.3 | 1.2 | 1.0 | 0.9 | 1.0 | 1.0 | 1.1 | 0.8 | 1.3 | 1.4 | 0.6 | 1.1 |
| HP 10 μg/ml | 0.5 | 0.3 | 0.1 | 0.4 | n.d. | 0.4 | 0.4 | n.d. | 0.1 | 0.3 | 0.1 | n.d. | 0.4 | 0.1 | 0.1 |
| HP 5 μg/ml | 0.7 | 0.6 | 0.4 | 0.5 | 0.0 | 0.9 | 0.7 | 0.0 | 0.2 | 0.8 | 0.4 | 0.6 | 0.5 | 0.2 | 0.3 |
| HP 0.5 μg/ml | 0.8 | 0.9 | 0.3 | 1.3 | 0.7 | 1.1 | 1.1 | 1.3 | 1.3 | 0.9 | 0.9 | 1.2 | 1.0 | 0.6 | 1.0 |
D1, D2, D3, D4, D5: donor 1 to donor 5;
Positive controls (PC): 50 μM omeprazole (1A2); 1 mM phenobarbital (2B6, 2C9); 100 mM ethanol (2E1); 10 μM rifampicine (3A4);
n.d. not detectable