Effects of chemical and antibody inhibitors of cytochrome P450 isoforms on TSU-68 hydroxylation by pooled human liver microsomes
The chemical and antibody inhibitors were preincubated with TSU-68 (50 μM) and human liver microsomes (1 mg of protein/ml) at 37°C for 5 and 30 min, respectively.
Inhibitor | Concentration or Volume | Residual Activity | ||||
|---|---|---|---|---|---|---|
| M1 | M2 | M3 | ||||
| % control | ||||||
| Chemical inhibitor | ||||||
| α-Naphthoflavone (CYP1A2) | 1 μM | 21 | 19 | 26 | ||
| 10 μM | 9 | 21 | 23 | |||
| Quercetin (CYP2C8) | 10 μM | 63 | 72 | 67 | ||
| 30 μM | 40 | 47 | 45 | |||
| Quinidine (CYP2D6) | 4 μM | 98 | 115 | 97 | ||
| 40 μM | 88 | 146 | 91 | |||
| Ketoconazole (CYP3A4) | 1 μM | 104 | 115 | 109 | ||
| 2 μM | 103 | 113 | 105 | |||
| Antibody inhibitor | ||||||
| Anti-CYP1A2 | 20 μl | 8 | 4 | 7 | ||
| 40 μl | 3 | 2 | 4 | |||
| Anti-CYP2C8 | 20 μl | 96 | 102 | 96 | ||
|
| 40 μl | 94 | 101 | 95 | ||