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The natural flavones, acacetin and apigenin, induce Cdk-Cyclin mediated G2/M phase arrest and trigger ROS-mediated

Anil Khushalrao Shendge1, Dipankar Chaudhuri1, Nripendranath Mandal2

  • 1Division of Molecular Medicine, Bose Institute, P-1/12 CIT Scheme - VIIM, Kolkata, West Bengal, 700054, India.

Molecular Biology Reports
|January 4, 2021
PubMed

Insights

Acacetin and apigenin flavonoids show potent anticancer activity against glioblastoma cells (U87). These compounds induce cell death via ROS generation, cell cycle arrest, and apoptosis, offering potential therapeutic strategies for brain cancer.

Area of Science:

  • Oncology
  • Biochemistry
  • Molecular Biology

Background:

  • Glioblastoma is an aggressive brain cancer with a poor prognosis.
  • Flavonoids like acacetin and apigenin are plant-derived compounds with potential therapeutic properties.

Purpose of the Study:

  • To investigate the anticancer effects of acacetin and apigenin on glioblastoma U87 cells.
  • To elucidate the underlying mechanisms of their cytotoxic and apoptotic activities.

Main Methods:

  • Isolation of acacetin and apigenin.
  • Cytotoxicity assays (IC50 determination).
  • Flow cytometry for cell cycle analysis and apoptosis detection (Annexin-V/DAPI).
  • ROS detection (DCFH-DA staining).
  • Western blotting for apoptosis and cell cycle regulatory proteins (Bax, t-Bid, caspases, p21, Cyclins, Cdk-1).

Main Results:

  • Acacetin and apigenin exhibited selective cytotoxicity against U87 cells (IC50 values provided).
  • Compounds induced G2/M cell cycle arrest and increased sub-G1 population, indicating apoptosis.
  • ROS generation was observed, contributing to cell cycle arrest and apoptosis.
  • Western blotting confirmed apoptosis pathway activation (intrinsic for acacetin, both intrinsic and extrinsic for apigenin) and G2/M arrest mechanisms.

Conclusions:

  • Acacetin and apigenin demonstrate significant anticancer effects on glioblastoma cells.
  • ROS induction is a key mechanism mediating their cytotoxic and apoptotic effects.
  • These flavonoids hold promise as potential therapeutic agents for glioblastoma treatment.
Keywords:
FlavonoidsMedicinal plantsROS-inductionU87 cell lineanticancer activitycaspase-cascade pathway

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