Magnesium isoglycyrrhizinate ameliorates high fructose-induced liver fibrosis in rat by increasing miR-375-3p to suppress JAK2/STAT3 pathway and TGF-β1/Smad signaling

Acta Pharmacol Sin. 2019 Jul;40(7):879-894. doi: 10.1038/s41401-018-0194-4. Epub 2018 Dec 19.

Abstract

Increasing evidence has demonstrated that excessive fructose intake induces liver fibrosis. Epithelial-mesenchymal transition (EMT) driven by transforming growth factor-β1 (TGF-β1)/mothers against decapentaplegic homolog (Smad) signaling activation promotes the occurrence and development of liver fibrosis. Magnesium isoglycyrrhizinate is clinically used as a hepatoprotective agent to treat liver fibrosis, but its underlying molecular mechanism has not been identified. Using a rat model, we found that high fructose intake reduced microRNA (miR)-375-3p expression and activated the janus-activating kinase 2 (JAK2)/signal transducer and activator of transcription 3 (STAT3) cascade and TGF-β1/Smad signaling, which is consistent with the EMT and liver fibrosis. To further verify these observations, BRL-3A cells and/or primary rat hepatocytes were exposed to high fructose and/or transfected with a miR-375-3p mimic or inhibitor or treated with a JAK2 inhibitor, and we found that the low expression of miR-375-3p could induce the JAK2/STAT3 pathway to activate TGF-β1/Smad signaling and promote the EMT. Magnesium isoglycyrrhizinate was found to ameliorate high fructose-induced EMT and liver fibrosis in rats. More importantly, magnesium isoglycyrrhizinate increased miR-375-3p expression to suppress the JAK2/STAT3 pathway and TGF-β1/Smad signaling in these animal and cell models. This study provides evidence showing that magnesium isoglycyrrhizinate attenuates liver fibrosis associated with a high fructose diet.

Keywords: EMT; JAK2/STAT3 pathway; MicroRNA-375-3p; TGF-β1/Smad signaling; excessive fructose intake; magnesium isoglycyrrhizinate.

MeSH terms

  • Animals
  • Cell Line
  • Epithelial-Mesenchymal Transition / drug effects
  • Fructose
  • Janus Kinase 2 / metabolism
  • Liver Cirrhosis / chemically induced
  • Liver Cirrhosis / drug therapy*
  • Male
  • MicroRNAs / metabolism*
  • Rats, Sprague-Dawley
  • STAT3 Transcription Factor / metabolism
  • Saponins / pharmacology
  • Saponins / therapeutic use*
  • Signal Transduction / drug effects*
  • Smad Proteins, Receptor-Regulated / metabolism
  • Transforming Growth Factor beta1 / metabolism
  • Triterpenes / pharmacology
  • Triterpenes / therapeutic use*

Substances

  • 18alpha,20beta-hydroxy-11-oxo-norolean-12-en-3beta-yl-2-O-beta-D-glucopyranurosyl-alpha-D-glucopyranosiduronate magnesium tetrahydrate
  • MIRN375 microRNA, rat
  • MicroRNAs
  • STAT3 Transcription Factor
  • Saponins
  • Smad Proteins, Receptor-Regulated
  • Stat3 protein, rat
  • Transforming Growth Factor beta1
  • Triterpenes
  • Fructose
  • Jak2 protein, rat
  • Janus Kinase 2