Identification of the pig constitutive androstane receptor (pgCAR) agonist using a high-throughput screening assay

Abstract

Pigs are encountering a large number of xenobiotics potentially harmful consequences, which is not only bad for animal health and pork quality but also bad for human health. Therefore, identification of the Pig Constitutive Androstane Receptor (pgCAR) agonist would be beneficial for pigs and consumer, because of its pivotal role in xenobiotics-metabolism. In this study, A stable and sensitive cell-based high throughput screening (HTS) model is conducted in a 48-well format using the human hepatoma HepG2 cells transiently transfected with pcDNA3.1-pgCAR plasmid and reporter plasmids to identify chemicals or natural compounds that would promote CAR,and calibrated with reference pgCAR agonist, phenytoin. In conclusion, three active ingredients including Vitamin C, Folate and Sitosterol, were picked out as agonists by the high-throughput screening from 13 compounds, particularly the effects of Sitosterol.