Effects of fibrates and known inhibitors of metabolizing enzymes on SVA metabolism in human hepatocytes
| SVA Metabolite | % of Control (Mean ± S.D. n = 3–5) | |||||
|---|---|---|---|---|---|---|
| 75 μM GFZ | 75 μM Fenofibrate | 100 μM BOA | 1 μM Ketoconazole | 50 μM Troleandomycin | 20 μM Sulfaphenazole | |
| 3′-Hydroxy | 86 ± 12 | 96 ± 20 | 80 ± 3 | 21 ± 3 | 30 ± 3 | 85 ± 12 |
| Dihydrodiol | 84 ± 12 | 97 ± 11 | 98 ± 4 | 28 ± 15 | 38 ± 2 | 80 ± 3 |
| B1 | 99 ± 18 | 126 ± 23 | 6 ± 1 | 102 ± 15 | 92 ± 6 | 120 ± 25 |
| B2 | 90 ± 12 | 120 ± 17 | 8 ± 3 | 114 ± 16 | 100 ± 2 | 121 ± 26 |
| B3 | 108 ± 30 | 105 ± 20 | 3 ± 1 | 111 ± 17 | 70 ± 18 | 91 ± 16 |
| B3-Glucuronide | 19 ± 10 | 108 ± 25 | 2 ± 2 | 89 ± 10 | 95 ± 10 | 114 ± 30 |
| SV | 41 ± 15 | 92 ± 31 | 45 ± 3 | 189 ± 54 | 160 ± 5 | 105 ± 25 |
Results are expressed as percentage of control values (means ± S.D. n = 3–5 hepatocyte preparations), and were obtained following co-incubation of SVA (20 μM) and inhibitors at 37°C for 60 min with human hepatocytes (3 × 106cells/ml).