Fig. 4

Activity of each CYP in the Caco-2 4CYPs-MAC cells. a The metabolic activity of each CYP in Caco-2 4CYPs-MAC cells. The relative activity for each CYP was measured by comparing the parental Caco-2 cells and the Caco-2 4CYPs-MAC #2 (mean ± S.E., n = 3). b Permeability test using MDZ. The permeability test was performed 23 d after seeding Caco-2 cells and Caco-2 4CYPs-MAC #2, whereby 3 μM MDZ was added to the apical side, and after 30 min, the apical, intracellular, and basal supernatants were collected. The 1′-OH MDZ in the supernatant was measured through LC-MS/MS. c CYP3A4 inhibition test. Ketoconazole, an inhibitor of CYP3A4, was added to the Caco-2 4CYPs-MAC #2 and incubated for 1 h. A luminescent substrate was measured to detect CYP3A4 activity with different concentrations of ketoconazole