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Gamabufotalin Suppresses Colorectal Cancer Growth via Oxidative Stress-Induced Apoptosis and DNA Synthesis Inhibition

Hui Nie1, Anfang Cui2, Zhicheng Sun3

  • 1School of Pharmacy, Shandong First Medical University (Shandong Academy of Medical Sciences), Jinan, China.

Iranian Journal of Pharmaceutical Research : IJPR
|May 20, 2026
PubMed
Abstract

Insights

Gamabufotalin (GA) shows potent anti-colorectal cancer (CRC) activity by inducing cell death and halting proliferation. This compound effectively suppresses tumor growth in vivo with minimal toxicity, offering a promising new therapeutic avenue.

Area of Science:

  • Oncology
  • Pharmacology
  • Molecular Biology

Background:

  • Colorectal cancer (CRC) remains a leading cause of cancer mortality globally.
  • There is a critical need for novel, effective, and less toxic therapeutic agents for CRC.
  • Gamabufotalin (GA), a bufadienolide, exhibits potential antitumor activity, but its mechanisms in CRC require elucidation.

Purpose of the Study:

  • To investigate the therapeutic efficacy of Gamabufotalin (GA) against colorectal cancer (CRC).
  • To explore the underlying molecular mechanisms of GA's action in CRC.

Main Methods:

  • Utilized in vitro assays (cell viability, colony formation, EdU, cell cycle, apoptosis, ROS, mitochondrial potential) and in vivo xenograft models.
  • Integrated transcriptomic and proteomic profiling to identify molecular targets.
  • Validated GA's efficacy and toxicity in a nude mouse model.

Main Results:

  • GA demonstrated potent, dose-dependent anti-CRC activity in vitro (IC50: 24-30 nM) with high selectivity.
  • GA induced mitochondrial apoptosis via reactive oxygen species (ROS) generation and cell cycle arrest, inhibiting DNA synthesis.
  • Omics analysis revealed TP53I3/PIG3 upregulation and RFC3/NUCKS1 downregulation as key mechanisms.
  • GA suppressed tumor growth in vivo without observable systemic toxicity.

Conclusions:

  • Gamabufotalin (GA) selectively and potently inhibits CRC via ROS-mediated apoptosis and proliferation suppression.
  • GA possesses a favorable therapeutic index and defined molecular targets.
  • GA presents a promising therapeutic candidate for colorectal cancer treatment.
Keywords:
ApoptosisColorectal CancerDNA SynthesisGamabufotalinOxidative Stress

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