Table 4.
Ki values for the inhibition of CYP1A2-mediated phenacetin O-deethylatoin, CYP2C19-mediated S-mephenytoin 4-hydroxylation, CYP2E1-mediated chlorzoxazone 6-hydroxylation, CYP3A-mediated nifedipine dehydrogenation, CYP3A-mediated midazolam hydroxylation, and UGT1A1-mediated SN-38 glucuronidation activities in human liver microsomes by trans- and cis-resveratrol.
| Enzyme | Substrate | trans-Resveratrol | cis-Resveratrol | ||||||
|---|---|---|---|---|---|---|---|---|---|
| Without Preincubation |
With Preincubation (30 min) |
Without Preincubation |
With Preincubation (30 min) |
||||||
| Ki (μM) | Mode of Inhibition |
Ki (μM) | Mode of Inhibition |
Ki (μM) | Mode of Inhibition |
Ki (μM) | Mode of Inhibition |
||
| CYP1A2 | Phenacetin | 13.8 ± 1.70 | Competitive | 1.62 ± 0.11 | Noncompetitive | 9.19 ± 1.41 | Competitive | 9.46 ± 0.63 | Noncompetitive |
| CYP2C19 | S-Mephenytoin | - | - | 9.78 ± 0.60 | Noncompetitive | - | - | 21.8 ± 6.10 | Noncompetitive |
| CYP2E1 | Chlorzoxazone | - | - | 9.11 ± 1.62 | Competitive | - | - | 8.08 ± 1.43 | Competitive |
| CYP3A | Nifedipine | 23.6 ± 1.90 | Noncompetitive | 4.60 ± 0.11 | Noncompetitive | - | - | - | - |
| Midazolam | 23.8 ± 2.30 | Noncompetitive | 1.02 ± 0.22 | Uncompetitive | - | - | - | - | |
| UGT1A1 | SN-38 * | 27.4 ± 3.60 | Noncompetitive | - | - | - | |||
* SN-38: 7-Ethyl-10-hydroxycamptothecin.