Table 2.
Basal CYP activities.
Basal CYP activities pmol/h/50,000 cells | ||||
---|---|---|---|---|
HepG2 cells | HepaRG cells | 2D-cultured PHH | 3D-cultured PHH | |
CYP1A2 | nd | (0.46 ± 0.02) | (0.09 ± 0.01) | 0.22 ± 0.02 |
0.932 | ||||
CYP2B6 | nd | 0.33 ± 0.02 | 0.54 ± 0.04 | 2.11 ± 0.07 |
0.999 | 0.905 | 0.985 | ||
CYP2C9 | nd | (0.11 ± 0.01) | (0.016 ± 0.002) | 0.16 ± 0.01 |
0.854 | ||||
CYP2C19 | 0.16 ± 0.01 | 18.5 ± 1.0 | 0.47 ± 0.04 | 3.7 ± 0.1 |
0.976 | 0.939 | 0.815 | 0.978 | |
CYP2D6 | nd | 0.69 ± 0.06 | 0.25 ± 0.01 | 6.2 ± 0.3 |
0.823 | 0.950 | 0.935 | ||
CYP3A4 | 0.64 ± 0.04 | 85.6 ± 4.5 | 27.4 ± 1.5 | 60.4 ± 1.5 |
0.645 | 0.991 | 0.903 | 0.993 |
Basal CYP activity in HepG2, HepaRG, 2D-, and 3D-cultured primary cryopreserved human hepatocytes (PHH). Primary human hepatocytes used for 2D- and 3D-cultures were from the same batch of cryopreserved cells. Values presented are the metabolite formation rates (see Figure 2) and the corresponding regression coefficients (r2) of the metabolite-time curves. Metabolite concentrations were determined by LC-MS/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 (i.e., lacking basal activity).