Enzyme activity in colon slices after 0 and 24 h of incubation Activities are expressed as mean ± S.E.M.
Metabolite (Enzyme Involved) | Activity 0–3 ha | Activity 24–27 ha | % Initial Metabolic Rate after 24-h Preincubation | |
|---|---|---|---|---|
| pmol/mg protein/min | ||||
| 1-Hydroxymidazolam (CYP3A4/5) | ND | ND | ||
| 4-Hydroxydiclofenac (CYP2C9) | ND | ND | ||
| 1-Hydroxybufuralol (CYP2D6) | ND | ND | ||
| 7-HC (mainly CYP1A1) | ND | ND | ||
| 7-HC-GLUC (UGT1A6) | 247 ± 23 | 247 ± 37 | 100 | |
| 7-HC-SULF (SULT) | 49 ± 10 | 50 ± 13 | 100 | |
ND, not detectable; 7-HC-SULF, 7-hydroxycoumarin-sulfate; SULT, sulfotransferase
↵ a Lower limits of quantitation were 5 nM for 1-hydroxymidazolam, 4-hydroxydiclofenac, and 1-hydroxybufuralol and <0.25 μM for 7-HC and 7-HC-GLUC and 7-HC-SULF