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. Author manuscript; available in PMC: 2014 Sep 1.
Published in final edited form as: Pharm Res. 2013 Jul 30;30(9):2199–2208. doi: 10.1007/s11095-013-1101-9

Figure 1. Carapin, santonin and isokobusone activated the human and rat PXR.

Figure 1

(A) Chemical structures of carapin, santonin and isokobusone, along with those of the typical PXR and CAR agonists rifampicin, PCN, TCPOBOP, and CITCO. (B and C) CV-1 cells were cotransfected with the tk-CYP3A23-Luc reporter gene, together with the wild-type and mutant hPXR (B) or rPXR (C). Transfected cells were treated with the vehicle or the indicated compounds (10 μM each) for 24 h before luciferase assay. Rifampicin (RIF) and prenenolon-16α-carbonitrile (PCN) were included as the positive control ligands for hPXR and rPXR, respectively. Results are shown as fold induction over vehicle control and represent the average from triplicate assays. *, P < 0.05, vs the vehicle control group of each WT and mutant receptors.