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Journal of Natural Medicines

, Volume 70, Issue 3, pp 584–591 | Cite as

Epigallocatechin gallate inhibits hepatitis B virus via farnesoid X receptor alpha

  • Jun XuEmail author
  • Weizhen Gu
  • Chaoyan Li
  • Xiao Li
  • Guozhen Xing
  • Yan Li
  • Yanhui Song
  • Wenming Zheng
Original Paper

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.

Keywords

EGCG Binding FXRα HBV promoter 

Notes

Acknowledgments

The authors would like to thank Dr. Hualin Wang and Dr. Ningshao Xia for providing the HepG2-N10 cells. This work was supported by grants from the National Natural Science Foundation of China (NSFC) (No. 31201332), the Foundation of He’nan Educational Committee (No. 12B230007), and the Project of the Henan Province (Nos. 112300410088, 112102310324, and 132102310033).

Compliance with ethical standards

Conflict of interest

There is no conflict of interest to be declared by the authors.

Supplementary material

11418_2016_980_MOESM1_ESM.doc (32 kb)
Supplementary material 1 (DOC 32 kb)

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Copyright information

© The Japanese Society of Pharmacognosy and Springer Japan 2016

Authors and Affiliations

  • Jun Xu
    • 1
    Email author
  • Weizhen Gu
    • 1
  • Chaoyan Li
    • 1
  • Xiao Li
    • 1
  • Guozhen Xing
    • 1
  • Yan Li
    • 1
  • Yanhui Song
    • 2
  • Wenming Zheng
    • 1
  1. 1.College of Life SciencesHenan Agricultural UniversityZhengzhouChina
  2. 2.Department of Clinical LaboratoryThe First Affiliated Hospital of Soochow UniversitySuzhouChina

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