Table 3.
Induced CYP activities (20μM rifampicin) pmol/h/50,000 cells | ||||
---|---|---|---|---|
HepG2 cells | HepaRG cells | 2D-cultured PHH | 3D-cultured PHH | |
CYP1A2 | nd | (0.51 ± 0.04) | (0.09 ± 0.01) | 0.46 ± 0.02 |
0.956 | ||||
CYP2B6 | nd | 1.31 ± 0.04 | 1.7 ± 0.1 | 5.7 ± 0.1 |
0.998 | 0.975 | 0.994 | ||
CYP2C9 | nd | (0.12 ± 0.02) | (0.022 ± 0.002) | 0.41 ± 0.01 |
0.985 | ||||
CYP2C19 | 0.21 ± 0.01 | 75.9 ± 1.8 | 1.96 ± 0.11 | 30.7 ± 1.7 |
0.979 | 0.996 | 0.978 | 0.980 | |
CYP2D6 | nd | 3.9 ± 0.2 | 0.35 ± 0.01 | 8.6 ± 0.4 |
0.992 | 0.928 | 0.952 | ||
CYP3A4 | 1.1 ± 0.1 | 675 ± 20 | 129 ± 8 | 432 ± 17 |
0.999 | 0.999 | 0.943 | 0.952 |
CYP activity in HepG2, HepaRG, 2D-, and 3D-cultured primary cryopreserved human hepatocytes (PHH) after treatment with 20 μM rifampicin for 72 h. Primary human hepatocytes used for 2D- and 3D-cultures were from the same batch of cryopreserved cells. Values presented are the metabolite formation rates and the regression coefficients (r2) of the metabolite-time curves after pre-treatment with rifampicin. Metabolite concentrations were determined by LC/MS. Data are presented as mean ± SEM of at least three independent experiments. Values in brackets are based on measurements of the last experimental time-point only, concentrations of all earlier time-points were below LLOQ. nd = not determinable (lacking basal activity).