Baicalein inhibits cell development, metastasis and EMT and induces apoptosis by regulating ERK signaling pathway in

Hang Lin1, Yi Hao1, Xiaoqing Wan1

  • 1Department of Orthopedics, Zhejiang Hospital, Hangzhou City, China.

Insights

Baicalein effectively inhibits osteosarcoma cell growth, migration, and invasion by inducing apoptosis and cell cycle arrest. This natural compound demonstrates significant anti-tumor effects in vitro and in vivo by regulating the ERK signaling pathway.

Area of Science:

  • Oncology
  • Pharmacology
  • Molecular Biology

Background:

  • Osteosarcoma is a highly aggressive primary bone tumor.
  • Baicalein, a natural flavonoid, exhibits known broad-spectrum anti-tumor properties.
  • Understanding baicalein's specific anti-osteosarcoma mechanisms is crucial for therapeutic development.

Purpose of the Study:

  • To elucidate the molecular mechanisms by which baicalein inhibits osteosarcoma progression.
  • To investigate the role of the ERK signaling pathway in baicalein's anti-osteosarcoma effects.
  • To evaluate the therapeutic potential of baicalein in both in vitro and in vivo osteosarcoma models.

Main Methods:

  • In vitro studies utilized MG-63 osteosarcoma cells treated with varying baicalein concentrations (0-100 μM).
  • Assays included MTT, clone formation, wound healing, Transwell invasion, cell cycle, apoptosis (Hoechst staining, flow cytometry), and Western blotting for protein analysis.
  • In vivo efficacy was assessed using a BALB/c-nude mouse model with tumor xenografts.

Main Results:

  • Baicalein demonstrated a dose-dependent inhibition of cell viability, proliferation, migration, and invasion, with an IC50 of 67.57 μM.
  • It induced G1 cell cycle arrest and apoptosis, decreasing key proteins (e.g., CDK2, Cyclin D1, Bcl-2, N-cadherin) and increasing others (e.g., p21, p27, cleaved caspase-3, Bax, E-cadherin).
  • Baicalein significantly reduced tumor weight and volume in vivo, correlating with decreased p-ERK/ERK expression.

Conclusions:

  • Baicalein effectively inhibits osteosarcoma cell proliferation, metastasis, and epithelial-mesenchymal transition (EMT).
  • It induces cell cycle arrest and apoptosis, primarily through the regulation of the ERK signaling pathway.
  • Baicalein exhibits significant anti-osteosarcoma activity, warranting further investigation as a potential therapeutic agent.

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