Preliminary study on Emodin alleviating alpha-naphthylisothiocyanate-induced intrahepatic cholestasis by regulation of liver farnesoid X receptor pathway

Int J Immunopathol Pharmacol. 2016 Dec;29(4):805-811. doi: 10.1177/0394632016672218. Epub 2016 Oct 5.

Abstract

The aim of this study is to investigate Emodin on alleviating intrahepatic cholestasis by regulation of liver farnesoid X receptor (FXR) pathway. Cell and animal models of intrahepatic cholestatis were established. Biochemical tests and histomorphology were performed. The messenger RNA (mRNA) and protein expression of FXR, small heterodimer partner (SHP), uridine diphosphate glucuronosyltransferase 2 family polypeptide B4 (UGT2B4), and bile salt export pump (BSEP) was detected. As a result, compared with the model group, the serum levels of biochemical test were significantly lower in the Emodin group (P <0.01). The histopathological changes were remitted significantly by Emodin treatment. In the model group, the mRNA and protein expression of FXR, SHP, UGT2B4, and BSEP was significantly lower than in the normal group in cell models (P <0.05). With Emodin intervention, the expression of FXR, SHP, UGT2B4, and BSEP was notably increased (P <0.05). In conclusion, Emodin plays a protective role in intrahepatic cholestasis by promoting FXR signal pathways.

Keywords: Emodin; farnesoid X receptor (FXR); intrahepatic cholestasis; α-naphthyl isothiocyanate.

Publication types

  • Letter

MeSH terms

  • 1-Naphthylisothiocyanate / pharmacology*
  • ATP Binding Cassette Transporter, Subfamily B, Member 11
  • ATP-Binding Cassette Transporters / metabolism
  • Animals
  • Cell Line
  • Cholestasis, Intrahepatic / chemically induced*
  • Cholestasis, Intrahepatic / drug therapy*
  • Cholestasis, Intrahepatic / metabolism
  • Emodin / pharmacology*
  • Female
  • Glucuronosyltransferase / metabolism
  • Humans
  • Liver / drug effects*
  • Liver / metabolism
  • Male
  • RNA, Messenger / metabolism
  • RNA-Binding Proteins / metabolism*
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Cytoplasmic and Nuclear / metabolism
  • Signal Transduction / drug effects*

Substances

  • ATP Binding Cassette Transporter, Subfamily B, Member 11
  • ATP-Binding Cassette Transporters
  • Abcb11 protein, rat
  • RNA, Messenger
  • RNA-Binding Proteins
  • Receptors, Cytoplasmic and Nuclear
  • nuclear receptor subfamily 0, group B, member 2
  • 1-Naphthylisothiocyanate
  • Glucuronosyltransferase
  • Emodin