Erinacerins, Novel Glioma Inhibitors from Hericium erinaceus, Induce Apoptosis of U87 Cells through Bax/Capase-2 Pathway

Anticancer Agents Med Chem. 2020;20(17):2082-2088. doi: 10.2174/1871520620666200804104243.

Abstract

Background: Glioma is the most common tumor of the central nervous system. Hericium erinaceus, which has been reported to have a variety of pharmacological activities, is a widely used Traditional Chinese Medicine (TCM), and also a kind of delicious food accepted by the public.

Methods and results: In this study, two new natural products, compounds 1 and 2, were isolated and identified from Hericium erinaceus. They were named erinacerin O and erinacerin P, respectively, after the structural identification, and their effects on human glioma cell line U87 were evaluated. Erinacerin P (2) exhibited obvious cytotoxicity on human glioma cell line U87. The IC50 value of 2 was 19.32μg/mL. The results showed that the apoptosis of U87 cells treated with 2 increased and the morphology of U87 cells altered significantly. Flow cytometry experiment showed that 2 could significantly increase the apoptosis rate of U87 cells and reduce DNA replication. Western blot results suggested the Bax/capase-3 pathway was involved in the U87 cell apoptosis induced by 2.

Conclusion: Erinacerin O and Erinacerin P are novel compounds obtained from Hericium erinaceus and Erinacerin P could be a potential novel glioma inhibitor.

Keywords: Hericium erinaceus; U87; apoptosis; cell viability; erinacerin; nuclear magnetic resonance.

MeSH terms

  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / isolation & purification
  • Antineoplastic Agents / pharmacology*
  • Apoptosis / drug effects
  • Caspase 2 / metabolism
  • Cell Proliferation / drug effects
  • Cell Survival / drug effects
  • Central Nervous System Neoplasms / drug therapy*
  • Central Nervous System Neoplasms / metabolism
  • Central Nervous System Neoplasms / pathology
  • Cysteine Endopeptidases / metabolism
  • Dose-Response Relationship, Drug
  • Drug Screening Assays, Antitumor
  • Glioma / drug therapy*
  • Glioma / metabolism
  • Glioma / pathology
  • Hericium / chemistry*
  • Humans
  • Molecular Structure
  • Structure-Activity Relationship
  • Tumor Cells, Cultured
  • bcl-2-Associated X Protein / antagonists & inhibitors
  • bcl-2-Associated X Protein / metabolism

Substances

  • Antineoplastic Agents
  • BAX protein, human
  • bcl-2-Associated X Protein
  • CASP2 protein, human
  • Caspase 2
  • Cysteine Endopeptidases