title: In vitro and in vivo anti-hepatitis B virus activities of the lignan nirtetralin B isolated from Phyllanthus niruri L.
abstract: BACKGROUND
  Nirtetralin B, a new lignan first reported by our team, is isolated from Phyllanthus niruri L. This plant has long been used in folk medicine for liver protection and antihepatitis B in many Asian countries. This study was designed to evaluate the anti-hepatitis B virus activity of nirtetralin B using HepG2.2.15 cells and duck hepatitis B virus (DHBV) infected ducks as in vitro and in vivo models.
  
  
  METHODS
  Nirtetralin B was isolated from Phyllanthus niruri L. (Euphorbiaceae) by extraction and chromatographic procedures and the anti-hepatitis B virus activity was evaluated both in vitro and in vivo. The human HBV-transfected liver cell line HepG2.2.15 was used in vitro assay. And the in vivo anti-hepatitis B virus activity was evaluated on the expression of HBV replication, HBsAg, HBeAg, ALT and AST on day 0, 7, 14, 17 after nirtetralin B was dosed intragastricly (i.g.) once a day for 14 days at the dosages of 25, 50 and 100mg/kg/day in the duck hepatitis B virus (DHBV) infected ducks.
  
  
  RESULTS
  In the human HBV-transfected liver cell line HepG2.2.15, nirtetralin B effectively suppressed the secretion of the HBV antigens in a dose-dependent manner with IC50 values for HBsAg of 17.4μM, IC50 values for HBeAg of 63.9μM. In DHBV-infected ducklings, nirtetralin B significantly reduced the serum DHBV DNA, HBsAg, HBeAg, ALT and AST. And analysis of the liver pathological changes confirmed the hepatoprotective effect of nirtetralin B.
  
  
  CONCLUSIONS
  The experimental data demonstrated that nirtetralin B exhibits anti-hepatitis B virus activity both in vitro and in vivo.
authors.affiliation: Department of Chemistry, Guangxi University, Nanning 530004, PR China.
authors.forename: Sheng
authors.initials: S
authors.lastname: Liu
authors.affiliation: Department of Chemistry, Guangxi University, Nanning 530004, PR China. Electronic address: wxwei@gxu.edu.cn.
authors.forename: Wanxing
authors.initials: W
authors.lastname: Wei
authors.affiliation: School of Chemistry and Chemical Engineering, Sun Yat-Sen University, Guangzhou 510275, PR China.
authors.forename: Yubin
authors.initials: Y
authors.lastname: Li
authors.affiliation: Guangxi Medical University, Nanning 530021, PR China.
authors.forename: Xing
authors.initials: X
authors.lastname: Lin
authors.affiliation: Guangxi Center for Animal Disease Control and Prevention, Nanning 530004, PR China.
authors.forename: Kaichuang
authors.initials: K
authors.lastname: Shi
authors.affiliation: Department of Chemistry, Guangxi University, Nanning 530004, PR China.
authors.forename: Xun
authors.initials: X
authors.lastname: Cao
authors.affiliation: Department of Chemistry, Guangxi University, Nanning 530004, PR China.
authors.forename: Min
authors.initials: M
authors.lastname: Zhou
mesh_terms: D000818:Animals; D000840:Anisoles / Q000008:administration & dosage / Q000302:isolation & purification / Q000494:pharmacology*; D000998:Antiviral Agents / Q000008:administration & dosage / Q000302:isolation & purification / Q000494:pharmacology*; D004149:Dioxoles / Q000008:administration & dosage / Q000302:isolation & purification / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004372:Ducks; D005260:Female; D056945:Hep G2 Cells; D006509:Hepatitis B / Q000188:drug therapy*; D006514:Hepatitis B Surface Antigens / Q000097:blood; D015611:Hepatitis B Virus, Duck / Q000187:drug effects; D006513:Hepatitis B e Antigens / Q000097:blood; D006515:Hepatitis B virus / Q000187:drug effects; D006801:Humans; D020128:Inhibitory Concentration 50; D017705:Lignans / Q000008:administration & dosage / Q000302:isolation & purification / Q000494:pharmacology*; D008297:Male; D008519:Medicine, Traditional; D029803:Phyllanthus / Q000737:chemistry*; D014779:Virus Replication / Q000187:drug effects
chemical_list: D000840:Anisoles; D000998:Antiviral Agents; D004149:Dioxoles; D006514:Hepatitis B Surface Antigens; D006513:Hepatitis B e Antigens; D017705:Lignans; C475933:nirtetralin
keywords: Antiviral therapy; Duck hepatitis B virus; Hepatitis B virus; Hepatoprotective effect; Nirtetralin B