Menthofuran inactivation assays for CYP1A2, CYP2D6, CYP2E1, and CYP3A4 activities
| Inactivation Assays | Menthofuran | Activity | |
|---|---|---|---|
| 0 min | 15 min | ||
| μM | % | ||
| CYP1A2 | 0 | 100 | 93 |
| 10 | 91 | 85 | |
| 100 | 86 | 82 | |
| CYP2D6 | 0 | 100 | 98 |
| 10 | 103 | 103 | |
| 100 | 89 | 96 | |
| CYP2E1 | |||
| Expressed CYP2E1 | 0 | 100 | 102 |
| 10 | 92 | 94 | |
| 100 | 82 | 85 | |
| Human liver microsomes | 0 | 100 | 105 |
| 10 | 103 | 101 | |
| 100 | 76 | 80 | |
| CYP3A4 | 0 | 100 | 100 |
| 10 | 102 | 95 | |
| 100 | 94 | 92 | |
Caffeine N3-demethylation was the probe for CYP2D6 activity, dextromethorphan O-demethylation for CYP2D6 activity, chlorzoxazone 6-hydroxylase for CYP2E1, and dextromethorphanN-demethylation for CYP3A4. Human liver (HL109) was used. Results are averages of duplicate runs, in which the difference in values was <5%.