Anti-hepatitis B Virus Activity of α-DDB-FNCG, a Novel Nucleoside-Biphenyldicarboxylate Compound In Vitro and In Vivo

DOI Web Site Web Site PubMed
  • Yang Qinghua
    Academy of Medical and Pharmaceutical Sciences, Zhengzhou University, China The College of Chemistry and Molecular Engineering, Zhengzhou University, China
  • Zhao Xuejie
    Academy of Medical and Pharmaceutical Sciences, Zhengzhou University, China
  • Yu Wenquan
    The College of Chemistry and Molecular Engineering, Zhengzhou University, China
  • He Wu
    The College of Chemistry and Molecular Engineering, Zhengzhou University, China
  • Fang Xianzhen
    Henan Center for Animal Disease Control and Prevention, China
  • Zang Limin
    Academy of Medical and Pharmaceutical Sciences, Zhengzhou University, China
  • Wan Na
    Academy of Medical and Pharmaceutical Sciences, Zhengzhou University, China
  • Wang Qingduan
    Academy of Medical and Pharmaceutical Sciences, Zhengzhou University, China
  • Zheng Liyun
    Academy of Medical and Pharmaceutical Sciences, Zhengzhou University, China
  • Chang Junbiao
    Academy of Medical and Pharmaceutical Sciences, Zhengzhou University, China The College of Chemistry and Molecular Engineering, Zhengzhou University, China

書誌事項

タイトル別名
  • Anti-hepatitis B Virus Activity of <i>α</i>-DDB-FNCG, a Novel Nucleoside-Biphenyldicarboxylate Compound In Vitro and In Vivo

この論文をさがす

抄録

A novel codrug, α-DDB-FNCG, was synthesized through coupling of α-biphenyl dimethyl dicarboxylate (α-DDB) and the nucleoside analogue FNCG, via an ester bond. The anti-HBV activity and hepatoprotective effects of this compound were investigated both in vitro and in vivo. In HBV-transfected HepG2.2.15 cell line, the secretion of HBsAg and HBeAg as well as the levels of extracellular and intracellular viral DNA were determined by ELISA and real-time fluorescent quantitative Polymerase Chain Reaction (FQ-PCR), respectively. In DHBV-infected ducks, the viral DNA levels in serum and liver were determined by FQ-PCR. In addition, the levels of alanine transaminase (ALT) and aspartate aminotransferase (AST) in both serum and liver were also examined. The improvement of ducks’ livers was evaluated by histopathological analysis. It has been demonstrated that α-DDB-FNCG could suppress the levels of HBV antigens and viral DNA in a time- and dose-dependent manner in the HepG2.2.15 cell line. Furthermore, this codrug could also significantly inhibit the viral DNA replication and reduce the ALT and AST levels in both serum and liver of DHBV-infected ducks, with improved hepatocellular architecture in drug-treated ducks. In short, these results suggest that α-DDB-FNCG could be a promising candidate for further development of new anti-HBV agents with hepatoprotective effects.

収録刊行物

キーワード

詳細情報 詳細情報について

問題の指摘

ページトップへ