Table 1 Isoforms tested, marker reactions, incubation conditions, and Km used in the inhibition study
From: In vitro inhibitory effect of obtusofolin on the activity of CYP3A4, 2C9, and 2E1
CYPs | Marker reactions | Substrate concentration (μM) | Protein concentration (mg/mL) | Incubation time (min) | Estimated Km (μM) | Inhibitors (μM) |
|---|---|---|---|---|---|---|
1A2 | phenacetin O-deethylation | 40 | 0.2 | 30 | 48 | 10 μM furafylline |
2A6 | coumarin 7-hydroxylation | 1.0 | 0.1 | 10 | 1.5 | 10 μM tranylcypromine |
3A4 | testosterone 6β-hydroxylation | 50 | 0.5 | 10 | 53 | 1 μM ketoconazole |
2C8 | paclitaxel 6α-hydroxylation | 10 | 0.5 | 30 | 16 | 5 μM montelukast |
2C9 | diclofenac 4′-hydroxylation | 10 | 0.3 | 10 | 13 | 10 μM sulphaphenazole |
2C19 | S-Mephenytoin 4-hydroxylation | 100 | 0.2 | 40 | 105 | 50 μM tranylcypromine |
2D6 | dextromethorphan O-demethylation | 25 | 0.25 | 20 | 4.8 | 10 μM quinidine |
2E1 | chlorzoxazone 6-hydroxylation | 120 | 0.4 | 30 | 126 | 50 μM clomethiazole |