Alleviation of hepatic fibrosis and autophagy via inhibition of transforming growth factor-β1/Smads pathway through shikonin

J Gastroenterol Hepatol. 2019 Jan;34(1):263-276. doi: 10.1111/jgh.14299. Epub 2018 Jul 10.

Abstract

Background and aim: Liver fibrosis is a worldwide clinical challenge during the progression of chronic liver disease to liver cirrhosis. Shikonin is extracted from the root of Lithospermum erythrorhizon with antioxidant, anti-inflammatory, anticancer, and wound-healing properties. The study aims to investigate the protective effect of shikonin on liver fibrosis and its underlying mechanism.

Methods: Two liver fibrosis models were established in male C57 mice by intraperitoneal injection of CCl4 or bile duct ligation. Shikonin was administered orally three times weekly at a dose of 2.5 or 5 mg/kg. Protein and mRNA expressions were assayed by quantitative real-time polymerase chain reaction, Western blotting, and immunohistochemical staining.

Results: Shikonin significantly inhibited activation of hepatic stellate cells and extracellular matrix formation by downregulating the transforming growth factor-β1 expression and maintaining the normal balance between metalloproteinase-2 and tissue inhibitor of metalloproteinase-1. Shikonin also decreased hepatic stellate cell energy production by inhibiting autophagy.

Conclusions: The results confirmed that shikonin attenuated liver fibrosis by downregulating the transforming growth factor-β1/Smads pathway and inhibiting autophagy.

Keywords: TGF-β1/Smads pathway; autophagy; liver fibrosis; shikonin.

MeSH terms

  • Alanine Transaminase / blood
  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
  • Anti-Inflammatory Agents, Non-Steroidal / therapeutic use
  • Aspartate Aminotransferases / blood
  • Autophagy / drug effects
  • Disease Models, Animal
  • Down-Regulation / drug effects
  • Extracellular Matrix / metabolism
  • Hepatic Stellate Cells / physiology
  • Liver Cirrhosis / metabolism*
  • Liver Cirrhosis / pathology
  • Liver Cirrhosis / prevention & control*
  • Male
  • Matrix Metalloproteinase 2 / metabolism
  • Mice
  • Mice, Inbred C57BL
  • Naphthoquinones / pharmacology*
  • Naphthoquinones / therapeutic use
  • Signal Transduction / drug effects
  • Smad Proteins, Receptor-Regulated / antagonists & inhibitors*
  • Tissue Inhibitor of Metalloproteinase-1 / metabolism
  • Transforming Growth Factor beta1 / antagonists & inhibitors*

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Naphthoquinones
  • Smad Proteins, Receptor-Regulated
  • Tgfb1 protein, mouse
  • Timp1 protein, mouse
  • Tissue Inhibitor of Metalloproteinase-1
  • Transforming Growth Factor beta1
  • shikonin
  • Aspartate Aminotransferases
  • Alanine Transaminase
  • Matrix Metalloproteinase 2
  • Mmp2 protein, mouse