Antiangiogenic effect of a selective 5-HT4 receptor agonist

Takeshi Nishikawa1, Nelson H Tsuno, Yasutaka Shuno

  • 1Department of Surgical Oncology, University of Tokyo, Tokyo, Japan. takn-tky@umin.ac.jp <takn-tky@umin.ac.jp>

Abstract

Insights

Mosapride citrate, a serotonin (5-HT4) agonist, demonstrated anti-angiogenic effects by inhibiting endothelial cell proliferation and migration. This suggests its potential as a novel anti-cancer therapeutic agent.

Area of Science:

  • Biomedical research
  • Pharmacology
  • Cancer biology

Background:

  • Serotonin (5-hydroxytryptamine, 5-HT) influences cell growth in various carcinomas.
  • 5-HT has complex effects on blood vessels via multiple 5-HT receptors.
  • Mosapride citrate is a selective 5-HT4 receptor agonist with known prokinetic properties.

Purpose of the Study:

  • To investigate the anti-angiogenic potential of mosapride citrate.
  • To evaluate mosapride citrate's effects on human umbilical vein endothelial cells (HUVECs) in vitro.

Main Methods:

  • Assessed HUVEC proliferation using MTS assay.
  • Performed apoptosis and cell cycle detection assays.
  • Investigated HUVEC adhesion, migration, and tube formation on Matrigel.

Main Results:

  • Mosapride citrate inhibited HUVEC proliferation via cell cycle arrest (G0/G1 phase), not apoptosis.
  • Significantly reduced HUVEC migration and tube-like structure formation.
  • Did not affect HUVEC adhesion to extracellular matrix proteins.

Conclusions:

  • Mosapride citrate exhibits in vitro anti-angiogenic activity.
  • Suggests potential application of mosapride citrate as a novel anti-cancer agent.

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