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Updated: May 25, 2025

Radiosensitivity of Cancer Stem Cells in Lung Cancer Cell Lines
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A Promising Resveratrol Analogue Suppresses CSCs in Non-Small-Cell Lung Cancer via Inhibition of the ErbB2 Signaling

Tanapon Soonthonsrima1,2, Ismail Dwi Putra2,3, Preeyaphan Phookphan1,2

  • 1Department of Pharmacology and Physiology, Faculty of Pharmaceutical Sciences, Chulalongkorn University, Bangkok 10330, Thailand.

Chemical Research in Toxicology
|February 25, 2025
PubMed

Insights

A novel resveratrol derivative, YI-12, effectively suppresses cancer stem cells (CSCs) by targeting the ErbB2 pathway. This compound shows potent anticancer activity and induces apoptosis, offering a promising new therapeutic strategy.

Area of Science:

  • Oncology
  • Medicinal Chemistry
  • Molecular Biology

Background:

  • Cancer stem cells (CSCs) drive tumor aggressiveness and proliferation.
  • The ErbB2 signaling pathway is a key target in cancer therapeutics.
  • Resveratrol (RES) derivatives show potential in targeting CSCs.

Purpose of the Study:

  • Synthesize novel RES derivatives to enhance anticancer properties.
  • Investigate the structure-activity relationships (SARs) of these derivatives.
  • Explore their capacity to suppress CSCs and identify molecular targets.

Main Methods:

  • Synthesis of novel O-benzyl-substituted 1,3-diphenylpropane derivatives.
  • Anticancer activity assessment against lung cancer cell lines (A549, H460).
  • Analysis of CSC markers (CD133, OCT4, β-catenin) and apoptosis induction.
  • Molecular docking and bioinformatic analysis to identify molecular targets.
  • Inhibition of downstream signaling pathways (PI3K/AKT).

Main Results:

  • YI-12 demonstrated potent anticancer activity and inhibited colony formation in lung cancer cells.
  • YI-12 decreased expression of CSC markers (CD133, OCT4, β-catenin) and induced apoptosis in CSC-rich spheroids.
  • Molecular docking identified ErbB2 as a high-affinity target for YI-12 (-6.709 kcal/mol).
  • YI-12 inhibited the PI3K/AKT signaling pathway downstream of ErbB2.

Conclusions:

  • The novel resveratrol derivative YI-12 effectively inhibits CSCs via the ErbB2 signaling pathway.
  • YI-12 exhibits significant anticancer properties, including apoptosis induction and CSC marker suppression.
  • YI-12 represents a promising lead compound for developing new anticancer therapies targeting CSCs.

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