Molecular Biological Mechanisms of Action of Chrysophanol in Hepatic Stellate Cells Activated by Hepatic B Virus X Based on Network Pharmacology

Intervirology. 2024;67(1):119-135. doi: 10.1159/000542355. Epub 2024 Dec 6.

Abstract

Introduction: Chrysophanol (Cho) is a natural anthraquinone with biological effects such as inducing ferroptosis and anticancer activity. The hepatitis B virus X protein (HBx) is essential for HBV replication. We aimed to identify the key pathways in HBx-induced hepatic stellate cell (HSC) activation and to characterize the potential mechanisms of action of Cho against liver fibrosis.

Methods: HSC-T6 cells were transfected with FLAG (control group) or FLAG-HBx (HBx group), and RNA sequencing and Western blotting analysis were conducted to assess the effects of HBx and Cho on specific molecular targets and signaling pathways.

Results: Gene ontology and pathway analyses indicated that the genes targeted by HBx participate in immunological responses, chemokine and cytokine activity, cell-substrate adhesion, extracellular matrix organization, growth factor binding, defense responses, and antigen processing and presentation. RNA-seq and Western blotting data revealed that HBx-activated HSC-T6 cells exhibited upregulated expression of mammalian target of rapamycin (mTOR), phosphorylated mTOR (p-mTOR), S6, phosphorylated S6 (p-S6), peroxisome proliferator-activated receptor (PPAR-α), phosphorylated-PPAR-α (p-PPAR-α), CYP27, α-smooth muscle actin (α-SMA), connective tissue growth factor (CTGF), and Integrin-β1, which was reversed after treatment with Cho. These results were also verified in a HBx-activated HSC-T6 and LX-2 cell model and thioacetamide-induced liver fibrosis mouse model.

Conclusions: Thus, our findings indicate that Cho ameliorates HBx-induced HSC activation and liver fibrosis via inhibition of the mTOR and PPARs signaling pathways, suggesting that Cho is a potential therapeutic for chronic liver inflammation-mediated diseases.

Keywords: Chrysophanol; Hepatitis B virus X protein; Liver fibrosis; Mammalian target of rapamycin; Peroxisome proliferator-activated receptor; Thioacetamide.

MeSH terms

  • Animals
  • Anthraquinones* / pharmacology
  • Cell Line
  • Hepatic Stellate Cells* / drug effects
  • Hepatic Stellate Cells* / metabolism
  • Hepatic Stellate Cells* / virology
  • Hepatitis B virus* / drug effects
  • Hepatitis B virus* / genetics
  • Hepatitis B virus* / physiology
  • Humans
  • Liver Cirrhosis* / drug therapy
  • Liver Cirrhosis* / virology
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Network Pharmacology*
  • Signal Transduction* / drug effects
  • TOR Serine-Threonine Kinases / metabolism
  • Trans-Activators* / genetics
  • Trans-Activators* / metabolism
  • Viral Regulatory and Accessory Proteins* / metabolism

Substances

  • Viral Regulatory and Accessory Proteins
  • hepatitis B virus X protein
  • Trans-Activators
  • Anthraquinones
  • chrysophanic acid
  • TOR Serine-Threonine Kinases

Grants and funding

This study was supported by a grant from the Ministry of Science and Technology of Taiwan (Grant No. 109-2320-B-303-004-MY3 to CYK); the Taipei Tzu Chi Hospital, Buddhist Tzu Chi Medical Foundation in New Taipei City (Grant No. TCRD-TPE-109-06, TCRD-TPE-110-38, TCRD-TPE-MOST-109-15, and TCRD-TPE-110-08); the Buddhist Tzu Chi Medical Foundation (Grant No. TCMMP111-01-02 to CFC); and translational research grants from the Tzu Chi and Academia Sinica Cooperation (Grant No. TCAS-108-01 to CFC); the Cathay General Hospital in Taipei (Grant No. CGH-MR-A11112 to CHL).