Table 2.
Inhibitory effects (IC50 values) of trans- and cis-resveratrol against nine cytochrome P450 isoforms (P450s) in HLMs (n = 3).
| P450 Enzyme |
Substrate | Trans-resveratrol (µM) | Cis-resveratrol (µM) | ||||
|---|---|---|---|---|---|---|---|
| Without Preincubation |
With Preincubation (30 min) |
IC50 Shift | Without Preincubation |
With Preincubation (30 min) |
IC50 Shift | ||
| 1A2 | Phenacetin | 12.9 ± 2.50 | 1.21 ± 0.20 | 10.80 | 14.0 ± 4.10 | 7.20 ± 0.50 | 1.90 |
| 2A6 | Coumarin | >50.0 | >50.0 | – | >50.0 | 48.3 ± 17.0 | – |
| 2B6 | Bupropion | 34.8 ± 7.20 | 40.1 ± 14.9 | 0.90 | 28.1 ± 13.9 | 32.8 ± 6.10 | 0.90 |
| 2C8 | Amodiaquine | >50.0 | 35.2 ± 6.40 | >1.40 | >50.0 | >50.0 | – |
| 2C9 | Diclofenac | 36.2 ± 3.30 | 23.8 ± 4.10 | 1.50 | >50.0 | >50.0 | – |
| 2C19 | S-Mephenytoin | 48.4 ± 10.9 | 8.13 ± 1.61 | 6.00 | 46.5 ± 16.1 | 19.8 ± 4.20 | 2.30 |
| 2D6 | Dextromethor-phan | >50.0 | 32.8 ± 3.20 | >1.50 | >50.0 | >50.0 | - |
| 2E1 | Chlorzoxazone | >50.0 | 9.82 ± 2.21 | >5.00 | >50.0 | 10.8 ± 2.90 | >4.60 |
| 3A | Midazolam | 29.2 ± 4.50 | 16.6 ± 4.00 | 1.80 | >50.0 | >50.0 | - |
| Nifedipine | 19.6 ± 2.30 | 5.62 ± 0.60 | 3.50 | >50.0 | >50.0 | - | |