Dual Effects of Ketoconazole cis-Enantiomers on CYP3A4 in Human Hepatocytes and HepG2 Cells
Figure 1
Effects of ketoconazole cis-enantiomers on CYP3A4 mRNA expression in HepG2 cells and human hepatocytes.
(i) HepG2 cells were seeded in 6-well plates and stabilized for 16 h. Experiments were performed in four consecutive cell passages. (ii) Primary human hepatocytes from three different donors (HH52, HH54 and Hep220770) were used. Cells were incubated for 24 h with RIF (10 µM), vehicle (DMSO; 0.1% v/v) and ketoconazole ((+), (−), (rac); 1 µM, 30 µM, 50 µM). RT-PCR analyses of CYP3A4 mRNA are shown. The data are the mean ± SD from triplicate measurements and are expressed as a fold induction over vehicle-treated cells. The data were normalized to GAPDH mRNA levels. An asterisk (*) indicates that the value is significantly different from the activity of vehicle-treated cells.