Chemical basis of pregnane X receptor activators in the herbal supplement Gancao (licorice).

ABSTRACT:

Background and aims

The herbal supplement Gancao, also known as licorice, belongs to the genus Glycyrrhiza and has been used worldwide for its hepatoprotective effect. Recent studies have raised concerns about potential herb-drug interactions associated with Gancao via pregnane X receptor (PXR)-mediated induction of hepatic cytochrome P450 3A4 (CYP3A4). The current work aimed to determine the phytochemicals in Gancao that activate PXR and induce CYP3A4.

Methods

DPX2 cells were used for cell-based PXR reporter assays. The phytochemicals in Gancao extract were identified using a metabolomics approach. The effects of PXR activators identified from in vitro studies were further investigated in PXR- and CYP3A4-humanized mouse models.

Results

Gancao was verifi

SUBMITTER: Cheng A 

PROVIDER: S-EPMC11791855 | biostudies-literature | 2022 Dec

REPOSITORIES: biostudies-literature