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. 2009 Jan 21;37(4):900–908. doi: 10.1124/dmd.108.025130

Fig. 4.

Fig. 4.

Concentration-dependent effects of cyclase inhibitor treatments on PXR-responsive reporter expression in HepG2 cells. HepG2 cells were transiently transfected with pSG5-hPXR1, XREM-CYP3A4-Luc, and pRL-CMV and then incubated for 24 h with medium alone or containing 10–8 to 3 × 10–5 M Ro 48-8071 (A) or with medium containing 0.1% DMSO or 10–8 to 10–5 M BIBX 79 or U18666A (B). After treatment, cells were harvested for measurement of firefly and Renilla luciferase activities. Normalized (firefly/Renilla) values are expressed as -fold changes ± S.D. (n = 3 wells/treatment group) relative to the appropriate negative control group (i.e., medium alone for Ro 48-8071; DMSO-treated for BIBX 79 and U18666A). Concentration-response data were fit to sigmoid relationships, and EC50 values with 95% confidence intervals (CIs) are shown. *, p < 0.05 and **, p < 0.01 versus negative control.