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Dual-Action NSAID-Gold(I) Alkynyl Hybrids for Synergistic Anti-Inflammatory and Anticancer Therapy of Colorectal

Javier Sáez1, Luis Vicente Herrera-Marcos2, María Jesús Rodríguez-Yoldi3,4

  • 1Departamento de Química Inorgánica, Instituto de Síntesis Química Y Catálisis Homogénea (ISQCH). Universidad de Zaragoza-C.S.I.C, Zaragoza 50009, Spain.

Inorganic Chemistry
|March 27, 2026
PubMed

Insights

New gold(I) complexes derived from NSAIDs show potent anti-colorectal cancer activity. These compounds target key cancer pathways, offering selective tumor cell killing with reduced toxicity to healthy cells.

Area of Science:

  • Medicinal Chemistry
  • Oncology
  • Nanotechnology

Background:

  • Colorectal cancer (CRC) is a significant global health issue driven by inflammation and redox imbalance.
  • Developing novel therapeutic agents with improved efficacy and selectivity is crucial for CRC treatment.

Purpose of the Study:

  • To design and synthesize novel NSAID-derived alkynyl gold(I) complexes for colorectal cancer intervention.
  • To evaluate the antiproliferative activity and selectivity of these complexes against colon cancer cells.

Main Methods:

  • Synthesis of eight new alkynyl gold(I) derivatives coordinated to JohnPhos-gold(I) fragments.
  • Assessment of antiproliferative activity against Caco-2/TC7 colon cancer cells and other cell lines.
  • Mechanistic studies including enzyme inhibition assays, ROS production, mitochondrial membrane potential, cell cycle analysis, and gene expression analysis.

Main Results:

  • NSAID-derived gold(I) complexes demonstrated potent antiproliferative activity against colon cancer cells, outperforming oxaliplatin.
  • The most active complex, [Au(L1)JP], selectively inhibited thioredoxin reductase (TrxR) and cyclooxygenase-2 (COX-2).
  • Complex 1 induced ROS overproduction, disrupted mitochondrial membrane potential, and caused G1-phase arrest, with reduced cytotoxicity in nonmalignant cells.

Conclusions:

  • NSAID-derived alkynyl gold(I) complexes represent promising multitarget agents for colorectal cancer.
  • These compounds offer a potential therapeutic strategy by combining disruption of cancer pathways with COX-2 modulation.
  • The observed selectivity suggests a favorable therapeutic window for these novel gold complexes.

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