Hesperetin derivative-7 inhibits PDGF-BB-induced hepatic stellate cell activation and proliferation by targeting Wnt/β-catenin pathway

Int Immunopharmacol. 2015 Apr;25(2):311-20. doi: 10.1016/j.intimp.2015.02.009. Epub 2015 Feb 17.

Abstract

Liver fibrosis results from a continuous wound-healing response of the liver to repeated injury. Hesperidin (HDN) is a naturally occurring flavanone glycoside, which is extracted from fruit peels of the genus citrus. Previous studies focused on the anti-inflammation, anti-tumor and anti-oxidant roles of HDN. However, the role of HDN in hepatic fibrosis is still unknown. Here, we evaluated the role of HDND-7, a derivative of HDN which has better water solubility and bioavailability, in the activation and proliferation of PDGF-BB-induced hepatic stellate cells (HSCs), then we investigated the anti-fibrotic effect of HDND-7 in CCl4-induced mouse model of liver fibrosis. The study aimed to determine whether HDND-7 could affect the survival of HSC-T6 in vitro, while evaluating its anti-fibrotic efficacy on CCl4-induced liver fibrosis in Kunming mice. Our results revealed that HDND-7 inhibited the proliferation and activation of PDGF-BB-treated HSC-T6 cells in a time- and dose-dependent manner. In addition, administration of HDND-7 significantly attenuated liver fibrosis, as evident by the dramatic down-regulation of α-smooth muscle actin (α-SMA) and type I collagen alpha-1 (Col1α1) in both mRNA and protein levels in vivo and in vitro. Furthermore, we also found that HDND-7 decreased the expression of β-catenin and the downstream proteins, cyclind1 and C-myc, indicating that HDND-7 may inhibit the activation and proliferation of PDGF-BB-induced HSC-T6 and attenuate liver fibrosis, at least in part, through targeting the Wnt/β-catenin signaling pathway. Hence HDND-7 might be employed as a promising natural supplement for liver fibrosis drug therapy.

Keywords: Activation; HDND-7; Proliferation; Wnt/β-catenin signaling.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Actins / genetics
  • Actins / metabolism
  • Animals
  • Apoptosis / drug effects
  • Becaplermin
  • Cell Cycle / drug effects
  • Cell Line
  • Cell Proliferation / drug effects
  • Cell Survival / drug effects
  • Collagen Type I / genetics
  • Collagen Type I / metabolism
  • Collagen Type I, alpha 1 Chain
  • Fibrosis
  • Hepatic Stellate Cells / drug effects*
  • Hepatic Stellate Cells / physiology
  • Hesperidin / analogs & derivatives*
  • Hesperidin / pharmacology*
  • Hesperidin / therapeutic use
  • Liver Diseases / drug therapy
  • Liver Diseases / metabolism
  • Liver Diseases / pathology
  • Male
  • Mice
  • Proto-Oncogene Proteins c-sis
  • Wnt Signaling Pathway / drug effects*

Substances

  • Actins
  • Collagen Type I
  • Collagen Type I, alpha 1 Chain
  • Proto-Oncogene Proteins c-sis
  • alpha-smooth muscle actin, mouse
  • smooth muscle actin, rat
  • Becaplermin
  • Hesperidin