Esculetin - hPXR Activation Experiment - 1 CSV JSON

In Vitro Nuclear Receptor Induction Experiment

Esculetin - hPXR Activation Experiment - 1

Induction was detected.  Cutoff used —

Not available 

esculetin

  • Pregnane X receptor (PXR)

Cell system PXR-transfected hepatic cells

Results

DPX2 cells were used for hPXR reporter assays. Effects of the identified compounds (10 µmol/L each) from Gancao extract on hPXR activation. Rifampicin (10 µmol/L) was used as the positive control.

Sample Compound measured Value Measurement Study sequence Additional information N replicates

Experimental Conditions

DPX2 cells (Puracyp, Inc; Carlsbad, CA, USA) were used for screening PXR activators, which were derived from HepG2 cells and stably transfected with hPXR and a luciferase-linked CYP3A4 promoter. The assays were conducted using a previously reported method with minor revisions. In brief, DPX2 cells were cultured in 96-well plates (5x10^5 cells/mL) for 24 h. Varying concentrations of Gancao extract or phytochemicals were prepared in a dosing medium and incubated with DPX2 cells for another 24 h. Rifampicin was used as a positive control for hPXR activation. All incubations were conducted in triplicate.

Luciferase activity (Reporter gene assay)

5x10^5 cells/mL in 96-well plates

48 hours