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Palonosetron, a 5-HT3 Receptor Antagonist, Induces G1 Cell Cycle Arrest and Autophagy in Gastric Cancer Cells

Young Chul Yoo1, Lin Lin1, Sihak Lee2

  • 1Department of Anesthesiology and Pain Medicine, Anesthesia and Pain Research Institute, Yonsei University College of Medicine, 50-1 Yonsei-ro, Seodaemun-gu, Seoul 03722, Republic of Korea.

International Journal of Molecular Sciences
|October 29, 2025
PubMed

Insights

Three serotonin 5-HT3 receptor antagonists inhibited gastric cancer cell growth. Palonosetron demonstrated significant anti-tumor effects by regulating cell cycle and immune responses, showing promise for gastric cancer treatment.

Area of Science:

  • Oncology
  • Pharmacology
  • Molecular Biology

Background:

  • Serotonin (5-hydroxytryptamine, 5-HT) signaling influences cancer progression via 5-HT1 and 5-HT2 receptors.
  • The therapeutic potential of 5-HT3 receptor antagonists in gastric cancer remains largely unexplored.

Purpose of the Study:

  • To investigate the anti-cancer effects of 5-HT3 receptor antagonists (ondansetron, palonosetron, ramosetron) on gastric cancer.
  • To evaluate the efficacy of palonosetron in gastric cancer cell lines and a xenograft mouse model.

Main Methods:

  • Utilized AGS and MKN-1 gastric cancer cell lines for in vitro assays.
  • Administered 5-HT3 receptor antagonists to assess cell proliferation, migration, and colony formation.
  • Conducted xenograft mouse studies to evaluate in vivo anti-tumor activity and cytokine modulation.

Main Results:

  • All three antagonists suppressed proliferation, migration, and colony formation in AGS cells.
  • Palonosetron induced G1 cell cycle arrest, autophagy, and altered key protein expression (p27, p53, LC3B, GSK3β).
  • In vivo, palonosetron significantly reduced tumor growth and modulated pro-inflammatory cytokines (TNF-α, IL-6, IL-1β).

Conclusions:

  • 5-HT3 receptor antagonists, particularly palonosetron, exhibit potent anti-gastric cancer activity.
  • Palonosetron's anti-tumor effects are mediated through G1 cell cycle arrest and immunomodulation.
  • Palonosetron warrants further preclinical investigation as a potential therapeutic agent for gastric cancer.
Keywords:
5-HT3 receptorG1 cell cyclegastric cancerpalonosetron

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