Schisandrol B promotes liver enlargement via activation of PXR and YAP pathways in mice

Phytomedicine. 2021 Apr:84:153520. doi: 10.1016/j.phymed.2021.153520. Epub 2021 Feb 17.

Abstract

Background: Schisandrol B (SolB) is one of the bioactive components from a traditional Chinese medicine Schisandra chinensis or Schisandra sphenanthera. It has been demonstrated that SolB exerts hepatoprotective effects against drug-induced liver injury and promotes liver regeneration. It was found that SolB can induce hepatomegaly but the involved mechanisms remain unknown.

Purpose: This study aimed to explore the mechanisms involved in SolB-induced hepatomegaly.

Methods: Male C57BL/6 mice were injected intraperitoneally with SolB (100 mg/kg) for 5 days. Serum and liver samples were collected for biochemical and histological analyses. The mechanisms of SolB were investigated by qRT-PCR and western blot analyses, luciferase reporter gene assays and immunofluorescence.

Results: SolB significantly increased hepatocyte size and proliferation, and then promoted liver enlargement without liver injury and inflammation. SolB transactivated human PXR, activated PXR in mice and upregulated hepatic expression of its downstream proteins, such as CYP3A11, CYP2B10 and UGT1A1. SolB also significantly enhanced nuclear translocation of PXR and YAP in human cell lines. YAP signal pathway was activated by SolB in mice.

Conclusion: These findings demonstrated that SolB can significantly induce liver enlargement, which is associated with the activation of PXR and YAP pathways.

Keywords: Schisandrol B; hepatomegaly; liver enlargement; pregnane X receptor; yes-associated protein.

MeSH terms

  • Adaptor Proteins, Signal Transducing / genetics
  • Adaptor Proteins, Signal Transducing / metabolism*
  • Animals
  • Cell Proliferation / drug effects
  • Chemical and Drug Induced Liver Injury / metabolism
  • Chemical and Drug Induced Liver Injury / pathology
  • Cyclooctanes / toxicity*
  • Dioxoles / toxicity*
  • Drugs, Chinese Herbal / adverse effects
  • Drugs, Chinese Herbal / chemistry
  • Gene Expression Regulation / drug effects
  • Hep G2 Cells
  • Hepatocytes / drug effects
  • Hepatocytes / metabolism
  • Hepatocytes / pathology
  • Hepatomegaly / chemically induced*
  • Hepatomegaly / metabolism
  • Hepatomegaly / pathology
  • Humans
  • Lignans / toxicity*
  • Liver / drug effects
  • Liver / pathology
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Organ Size / drug effects
  • Pregnane X Receptor / genetics
  • Pregnane X Receptor / metabolism*
  • Schisandra / chemistry
  • Signal Transduction / drug effects
  • Transcription Factors / genetics
  • Transcription Factors / metabolism*
  • YAP-Signaling Proteins

Substances

  • Adaptor Proteins, Signal Transducing
  • Cyclooctanes
  • Dioxoles
  • Drugs, Chinese Herbal
  • Lignans
  • NR1I2 protein, human
  • Pregnane X Receptor
  • Transcription Factors
  • YAP-Signaling Proteins
  • YAP1 protein, human
  • schizandrol B