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Epigallocatechin gallate inhibits hepatitis B virus via farnesoid X receptor alpha

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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.

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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).

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Authors and Affiliations

  1. College of Life Sciences, Henan Agricultural University, 95 Wenhua Road, Zhengzhou, 450002, China

    Jun Xu, Weizhen Gu, Chaoyan Li, Xiao Li, Guozhen Xing, Yan Li & Wenming Zheng

  2. Department of Clinical Laboratory, The First Affiliated Hospital of Soochow University, 188 Shizi Road, Suzhou, 215006, China

    Yanhui Song

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  1. Jun Xu
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  2. Weizhen Gu
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Correspondence to Jun Xu.

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Xu, J., Gu, W., Li, C. et al. Epigallocatechin gallate inhibits hepatitis B virus via farnesoid X receptor alpha. J Nat Med 70, 584–591 (2016). https://doi.org/10.1007/s11418-016-0980-6

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  • DOI: https://doi.org/10.1007/s11418-016-0980-6

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