Journal: Liver Research

Article Title: Chemical basis of pregnane X receptor activators in the herbal supplement Gancao (licorice) ☆

doi: 10.1016/j.livres.2022.11.007

Figure Lengend Snippet: Gancao extract activates hPXR. Cell-based hPXR reporter assays were conducted using DPX2 cells. (A) Effect of Gancao extract on hPXR activation. Gancao extract was diluted 100-fold. RIF (10 μmol/L) was used as a positive control for hPXR activation. (B) A dose-dependent hPXR activation by Gancao extract (100- to 1000-fold dilution). The data in control groups were set as 1. All data are expressed as means ± SEM ( n = 3). ∗∗ P < 0.01, ∗∗∗ P < 0.001, ∗∗∗∗ P < 0.0001 vs. control. Abbreviations: hPXR, human pregnane X receptor; RIF, rifampicin; SEM, standard error of the mean.

Article Snippet: 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.

Techniques: Activation Assay, Positive Control, Control

Journal: Liver Research

Article Title: Chemical basis of pregnane X receptor activators in the herbal supplement Gancao (licorice) ☆

doi: 10.1016/j.livres.2022.11.007

Figure Lengend Snippet: Screening of Gancao phytoconstituents for PXR activators. DPX2 cells were used for hPXR reporter assays. (A) Effects of the identified compounds (10 μmol/L each) from Gancao extract on hPXR activation. RIF (10 μmol/L) was used as a positive control. All data are expressed as means ± SEM ( n = 3). ∗∗ P < 0.01, ∗∗∗∗ P < 0.0001 vs. control (set as 1). (B) Dose responses of GZ, GA, and glabridin on hPXR activation. The data in RIF group at 100 μmol/L were set as 1. All data are expressed as means ( n = 3). Abbreviations: GA, glycyrrhetinic acid; GZ, glycyrrhizin; hPXR, human pregnane X receptor; RIF, rifampicin; SEM, standard error of the mean.

Article Snippet: 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.

Techniques: Activation Assay, Positive Control, Control

Journal: Cancer research

Article Title: Activation status of the Pregnane X Receptor (PXR) influences Vemurafenib availability in humanized mouse models

doi: 10.1158/0008-5472.CAN-15-1454

Figure Lengend Snippet: DPX2 cells were used to calculate the EC50 (8.13 μM) and EMAX (8.54-fold) for vemurafenib mediated trans-activation of PXR

Article Snippet: We tested the capacity of crystalline vemurafenib to activate a PXR-driven luciferase reporter construct in the DPX2 cell line (Puracyp Inc.).

Techniques: Activation Assay