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Sci Rep. 2016 Jun 17;6:28116. doi: 10.1038/srep28116.

Antiproliferation of berberine is mediated by epigenetic modification of constitutive androstane receptor (CAR) metabolic pathway in hepatoma cells.

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Department of Pharmacology, School of Basic Medical Sciences, Peking University, Beijing, 100191, China.
Medical and Healthy Analytical Center, Peking University, Beijing, 100191, China.
Department of Drug Metabolism &Pharmacokinetics, Biogen, Cambridge, Massachusetts, USA.
Department of Pharmaceutical Sciences, School of Pharmacy, University of Maryland, Baltimore, USA.


Constitutive androstane receptor (CAR) regulates hepatic xenobiotic and energy metabolism, as well as promotes cell growth and hepatocarcinogenesis. Berberine is an ancient multipotent alkaloid drug which derived from Coptis chinensis plants. Here we report that berberine is able to be cellular uptake and accessible to chromatin in human hepatoma HepG2 cells. Berberine induces more apoptosis, cell cycle arrest, but less ROS production in CAR overexpressed mCAR-HepG2 cells. Moreover, berberine inhibits expressions of CAR and its target genes CYP2B6 and CYP3A4. Furthermore, berberine enhances DNA methylation level in whole genome but reduces that in promoter regions CpG sites of CYP2B6 and CYP3A4 genes under the presence of CAR condition. These results indicated that the antiproliferation of berberine might be mediated by the unique epigenetic modifying mechanism of CAR metabolic pathway, suggesting that berberine is a promising candidate in anticancer adjuvant chemotherapy, due to its distinct pharmacological properties in clinic.

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