title: Epigallocatechin gallate inhibits hepatitis B virus via farnesoid X receptor alpha.
abstract: Plants possess various natural antiviral properties. Epigallocatechin-3-gallate (EGCG), a major component of green tea, inhibits a variety of viruses. However, the clinical application of EGCG is currently hindered by a scarcity of information on its molecular mechanism of action. In the present study, we examined the anti-HBV (hepatitis B virus) effects of catechins from green tea at the transcriptional and antigen-expression levels, as well as the associated molecular mechanisms, because HBV-associated liver diseases have become a key public health issue due to their serious impact on human physical and mental health. By using fluorescence quenching and affinity binding, we demonstrated that EGCG is an important transcriptional regulator of the HBV genome, which it achieves by interacting with farnesoid X receptor alpha (FXRα). Luciferase assay showed that EGCG effectively inhibited the transcription of the HBV promoter dose-dependently when expression plasmids of FXRα and retinoid X receptor α (RXRα) were co-transfected into HEK293 cells. These results indicate that the downregulation of the HBV antigen and the decrease in the transcriptional activation of the HBV EnhII/core promoter by FXRα/RXRα are mainly due to the interaction between EGCG and FXRα. Therefore, EGCG, an antagonist of FXRα in liver cells, has the potential to be employed as an effective anti-HBV agent.
authors.affiliation: College of Life Sciences, Henan Agricultural University, 95 Wenhua Road, Zhengzhou, 450002, China. xujun0828@126.com.
authors.forename: Jun
authors.initials: J
authors.lastname: Xu
authors.affiliation: College of Life Sciences, Henan Agricultural University, 95 Wenhua Road, Zhengzhou, 450002, China.
authors.forename: Weizhen
authors.initials: W
authors.lastname: Gu
authors.affiliation: College of Life Sciences, Henan Agricultural University, 95 Wenhua Road, Zhengzhou, 450002, China.
authors.forename: Chaoyan
authors.initials: C
authors.lastname: Li
authors.affiliation: College of Life Sciences, Henan Agricultural University, 95 Wenhua Road, Zhengzhou, 450002, China.
authors.forename: Xiao
authors.initials: X
authors.lastname: Li
authors.affiliation: College of Life Sciences, Henan Agricultural University, 95 Wenhua Road, Zhengzhou, 450002, China.
authors.forename: Guozhen
authors.initials: G
authors.lastname: Xing
authors.affiliation: College of Life Sciences, Henan Agricultural University, 95 Wenhua Road, Zhengzhou, 450002, China.
authors.forename: Yan
authors.initials: Y
authors.lastname: Li
authors.affiliation: Department of Clinical Laboratory, The First Affiliated Hospital of Soochow University, 188 Shizi Road, Suzhou, 215006, China.
authors.forename: Yanhui
authors.initials: Y
authors.lastname: Song
authors.affiliation: College of Life Sciences, Henan Agricultural University, 95 Wenhua Road, Zhengzhou, 450002, China.
authors.forename: Wenming
authors.initials: W
authors.lastname: Zheng
mesh_terms: D002392:Catechin / Q000031:analogs & derivatives* / Q000737:chemistry; D045744:Cell Line, Tumor; D056945:Hep G2 Cells; D006515:Hepatitis B virus / Q000737:chemistry*; D006801:Humans; D018160:Receptors, Cytoplasmic and Nuclear / Q000737:chemistry*; D013662:Tea / Q000737:chemistry*; D000099150:Receptor, Farnesoid X-Activated
chemical_list: D002392:Catechin; D018160:Receptors, Cytoplasmic and Nuclear; D013662:Tea; D000099150:Receptor, Farnesoid X-Activated; C045651:epigallocatechin gallate
keywords: Binding; EGCG; FXRα; HBV promoter