Table 2.
Decrease of progesterone (PGS) and atorvastatin (ATVS) lactone hydroxylation by DON in CYP3A4-containing nanodiscs (ND).
| Substrate (µM) | Without DON 1 | DON 1, 10 μM | DON 1, 49 μM |
|---|---|---|---|
| nmol/(min×nmol CYP3A4) | nmol/(min×nmol CYP3A4) | nmol/(min×nmol CYP3A4) | |
| PGS#, 15 μM | 5.3 ± 0.6 | 5.0 ± 0.6 | 4.1 ± 0.4 |
| PGS#, 40 μM | 10.4 ± 1.0 | 9.8 ± 0.9 | 8.9 ± 0.8 |
| ATVS lactone*, 8 μM | 2.8 ± 0.2/0.47 ± 0.08 | 2.7 ± 0.25/0.48 ± 0.08 | 2.7 ± 0.16/0.52 ± 0.06 |
| ATVS lactone*, 18 μM | 3.2 ± 0.2/1.1 ± 0.1 | 3.2 ± 0.2/0.97 ± 0.12 | 3.1 ± 0.18/0.87 ± 0.13 |
1 Data points are expressed as mean ± SEM (n = 3, with two technical replicates). #Formation rates were calculated for the sum of the hydroxylated metabolites 2β- and 6β-OH-PGS. * Formation rates were separately calculated for the hydroxylated metabolites 4-OH-ATVS lactone (major product) and 2-OH-ATVS lactone (minor product).