Identification of P450s involved in the metabolism of 17-OHPC
Mean ± S.D. of triplicate in vitro preparations. Amount of metabolite is expressed in terms of HPC equivalent. Significant levels of metabolite were detected on incubation of 17-OHPC (100 μM) with expressed CYP3A4/5, whereas no metabolite could be detected for other P450s.
Expressed P450s | Metabolite (M2HLM) Generated | 17-OHPC Metabolized |
|---|---|---|
| pmol/pmol P450/min | pmol/pmol P450/min | |
| CTRL | N.D. | N.D. |
| 1A1 | N.D. | N.D. |
| 1A2 | N.D. | N.D. |
| 1B1 | N.D. | N.D. |
| 2A6 | N.D. | N.D. |
| 2B6 | N.D. | N.D. |
| 2C8 | N.D. | N.D. |
| 2C9*1 | N.D. | N.D. |
| 2C9*2 | N.D. | N.D. |
| 2C9*3 | N.D. | N.D. |
| 2C18 | N.D. | N.D. |
| 2D6*1 | N.D. | N.D. |
| 2D6*10 | N.D. | N.D. |
| 2E1 | N.D. | N.D. |
| 19 | N.D. | N.D. |
| FMO1 | N.D. | N.D. |
| FMO3 | N.D. | N.D. |
| FMO5 | N.D. | N.D. |
| CYP3A4 | 27.4 ± 1.2 | 64.5 ± 0.1 |
| CYP3A5 | 57.1 ± 3.7 | 68.4 ± 0.4 |