- Natural product: Licorice (Glycyrrhiza glabra)
- Associated study: Chemical basis of pregnane X receptor activators in the herbal supplement Gancao (licorice)
In Vitro Nuclear Receptor Induction Experiment
Esculetin - hPXR Activation Experiment - 1
Induction was detected. Cutoff used —
Not available
- 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 |
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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