TABLE 3

Concentration response data for steroidal ligands activating human PXR in HepG2 cells

PXR activation in the HepG2 human liver cell line was determined by a luciferase-based reporter assay as described previously (Krasowski et al., 2005b). Each drug concentration was performed at least in quadruplicate and repeated in separate experiments for a total of at least three times. Data are expressed as mean ± S.D. For further experimental details, see Materials and Methods.


Compound Name

EC50

Efficacy
μM
17β-dihydroandrosterone 4.15 ± 0.2 0.68
Androstanol 6.27 ± 0.3 0.5
Dihydrotestosterone 11.4 ± 0.5 0.39
Etiocholanolone 5.7 ± 0.6 0.54
5β-Cholan-3α,7α,12α,24-tetrol >100 0
Taurochenodeoxycholic acida 104 ± 8 0.5
Deoxycholic acida 50.2 ± 4.5 0.19
Lithocholic acida 10 ± 0.1 0.15
7-Ketolithocholic acida 21.5 ± 1.4 0.58
12-Ketolithocholic acida 31.3 ± 5.8 0.86
ω-Muricholic acida >100 0
Taurocholic acida >100 0
Cholesterol >100 0
Estradiol 16 ± 0.1 0.34
Estrone 37.9 ± 3.3 0.47
Estriol >100 0
5β-Pregnane-3,20-dione 2.6 ± 0.2 0.97
17-Hydroxyprogesterone 17.7 ± 2.3 0.7
Petromyzonola >100 0
Allocholic acida >100 0
PCN >100 0
Cortolone 44.7 ± 7.4 0.72
Estetrol 2.14 ± 0.2 0.29
Epitestosterone sulfate 3.39 ± 0.7 0.67
5β-Pregnan-3α,20β,diol 3.81 ± 0.3 0.49
5α-Androstan-3β-ol 0.8 ± 0.01 0.43
16,(5α)-Androsten-3β-ol 4.77 ± 1.0 1.01
5β-Androstan-3α-ol 1.41 ± 0.1 1.12
Tauro-β-muricholic acida >100 0
Lithocholic acid acetatea
1.2 ± 0.2
0.54