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. 2012 Mar;165(5):1595–1608. doi: 10.1111/j.1476-5381.2011.01665.x

Figure 2.

Figure 2

Atorvastatin and its metabolites induce assembly of the human PXR-LBD and CYP3A4 promoter activity. (A) PXR-assembly assay in HepG2 cells, co-transfected with expression plasmids encoding GAL4-DBD/hPXR-LBD (132–188) and VP16-AD/hPXR-LBD (189–434) fusion proteins. Cells were treated for 40 h with 0.1% DMSO or increasing concentrations of the indicated compounds. Mean fold induction (±SD) of the respective normalized activity of co-transfected reporter plasmid pGL3-G5 by treatment with the indicated concentrations of compounds is shown. (B) and (C) HepG2-PXR cells were transfected with pGL3-CYP3A4(-7830/Δ7208–364) and treated with increasing concentrations (C) or with 30 µM of the indicated compounds (B) for 24 h. The columns (B) and graphs (C) show mean fold induction (±SD) of normalized CYP3A4 promoter reporter gene activity by treatment with compounds. The respective reporter activity of transfected cells, which were treated with DMSO only, was designated as 1. Data were analysed by repeated measures one-way anova with Bonferroni's multiple comparisons post–test. *P < 0.05, significant differences between groups as shown. RIF, rifampin; ATV, atorvastatin; ATV-L, atorvastatin lactone, o-OH-ATV, ortho-hydroxy atorvastatin; p-OH-ATV, para-hydroxy atorvastatin.