Effects of 8, 26, and 30 on human PXR activation.
(A) Dual-luciferase reporter gene assay
was performed in HEK293T cells transiently transfected with expression
vectors encoding human PXR (pSG5-hPXR), reporter plasmid (pGL3-CYP3A4-XREM-Luc),
and the control plasmid (pRL-TK). Cells were treated with the positive
agonist RIF (10 μM) or compounds 1–34 (10 μM) for
24 h. (B) Dose–response assay for 8, 26, 30, and RIF (0.1, 0.5, 1, 5, 10, and 50 μM).
Data are presented as mean ± SD (n = 3). *P < 0.05, **P < 0.01, ***P < 0.001, ****P < 0.0001, versus
the vehicle.