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Bavachinin inhibits cholesterol synthesis enzyme FDFT1 expression via AKT/mTOR/SREBP-2 pathway

Xi Dong1, Yue Zhu2, Shan Wang1

  • 1Beijing Key Laboratory of Innovative Drug Discovery of Traditional Chinese Medicine (Natural Medicine) and Translational Medicine, Institute of Medicinal Plant Development, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing, PR China; Key Laboratory of New Drug Discovery Based on Classic Chinese Medicine Prescription, Chinese Academy of Medical Sciences, Beijing, PR China; Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine, Ministry of Education, Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing, PR China; Key Laboratory of Efficacy Evaluation of Chinese Medicine Against Glycolipid Metabolic Disorders, State Administration of Traditional Chinese Medicine, Institute of Medicinal Plant Development, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing, PR China.

International Immunopharmacology
|August 23, 2020
PubMed

Insights

Bavachinin, derived from traditional Chinese medicine, protects liver cells from damage by inhibiting cholesterol synthesis. This compound shows potential as a future drug for non-alcoholic fatty liver disease (NAFLD).

Area of Science:

  • Biochemistry
  • Hepatology
  • Pharmacology

Background:

  • Non-alcoholic fatty liver disease (NAFLD) is a chronic liver condition with no approved treatments.
  • NAFLD pathogenesis involves lipid metabolism imbalance and hepatotoxicity.
  • Squalene synthase (SQS), encoded by FDFT1, is a key regulator of cholesterol synthesis and a potential therapeutic target for NAFLD.

Purpose of the Study:

  • To investigate bavachinin (BVC) from Fructus Psoraleae (FP) as a potential therapeutic agent for NAFLD.
  • To elucidate the mechanism by which BVC protects against palmitic acid-induced liver cell death.
  • To determine if BVC inhibits FDFT1 and impacts cholesterol synthesis via the AKT/mTOR/SREBP-2 pathway.

Main Methods:

  • HepaRG cells were used to assess the protective effects of BVC against palmitic acid-induced cell death.
  • Lipid accumulation and cholesterol synthesis were measured.
  • FDFT1 expression and activity were analyzed, including in cells with FDFT1 overexpression.
  • The AKT/mTOR/SREBP-2 pathway was investigated.

Main Results:

  • Bavachinin protected HepaRG cells from palmitic acid-induced death.
  • BVC suppressed lipid accumulation and cholesterol synthesis.
  • BVC inhibited FDFT1 activity through the AKT/mTOR/SREBP-2 pathway.
  • Overexpression of FDFT1 counteracted the inhibitory effects of BVC on cholesterol synthesis.

Conclusions:

  • Bavachinin acts as an inhibitor of cholesterol synthesis by targeting FDFT1 via the AKT/mTOR/SREBP-2 pathway.
  • Bavachinin demonstrates potential as a novel therapeutic agent for treating NAFLD.
Keywords:
BavachininCholesterol synthesis inhibitionFDFT1HMG-CoA synthaseSqualene synthase

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