Effects of CYP inhibitors (A) or anti-CYP-antibody (B) on the formation of M3 (unknown)
| A | B | ||||
|---|---|---|---|---|---|
| Chemical | Dose | Formation | Anti-Body (vehicle) | Dose | Formation |
| μM | % | mg protein/ml | % | ||
| Control | 100.0 ± 3.6 | Control (R) | 100.0 ± 12.1 | ||
| SKF525A | 40 | 28.7 ± 3.51-a | Control (G) | 100.0 ± 2.0 | |
| 200 | 11.6 ± 3.11-a | Control (T) | 100.0 ± 17.3 | ||
| α-Naphthoflavone | 0.2 | 91.3 ± 18.1 | Anti-CYP1A1/1A2 (R) | 1 | 89.9 ± 9.6 |
| 1 | 90.5 ± 19.2 | 2 | 94.9 ± 5.8 | ||
| Coumarine | 2 | 104.4 ± 6.6 | Anti-CYP2A6 (T) | 0.1 | 88.9 ± 20.0 |
| 10 | 94.9 ± 18.8 | 0.2 | 102.9 ± 22.9 | ||
| Quinidine | 1 | 100.5 ± 21.8 | Anti-CYP2B6 (T) | 0.1 | 101.5 ± 24.9 |
| 5 | 98.9 ± 10.7 | 0.2 | 94.9 ± 25.8 | ||
| Chlorzoxazone | 1 | 109.7 ± 21.2 | Anti-CYP2C (G) | 1 | 105.5 ± 2.2 |
| 5 | 97.6 ± 18.7 | 2 | 105.0 ± 5.1 | ||
| Sulphaphenazole | 1 | 92.8 ± 26.5 | Anti-CYP2D6 (R) | 1 | 94.2 ± 5.8 |
| 5 | 122.0 ± 19.5 | 2 | 97.8 ± 13.5 | ||
| Ketoconazole | 0.4 | 9.0 ± 4.31-a | Anti-CYP2E1 (T) | 0.1 | 97.3 ± 28.0 |
| 2 | 0.9 ± 0.31-a | 0.2 | 96.7 ± 20.4 | ||
| Anti-CYP3A4 (R) | 1 | 63.5 ± 18.31-a | |||
| 2 | 32.2 ± 13.31-a | ||||
CPT-11 (10 μM) was incubated with pooled human hepatic microsomes (1 mg of protein/ml) at 37°C for 10 min in the presence of an inhibitor or an antibody for CYP. Controls in antibody experiments were set for corresponding vehicles of rabbit serum (R), goat serum (G), and Tris buffer (T), respectively. The values represent the mean ± S.D. of data from triplicate experiments.
↵1-a p < 0.01 versus control.