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Gold(I) Complexes Based on Nonsteroidal Anti-Inflammatory Derivatives as Multi-Target Drugs against Colon Cancer

Javier Saez1, Javier Quero2,3, María Jesús Rodriguez-Yoldi2,3

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

Inorganic Chemistry
|October 10, 2024
PubMed

Insights

New gold(I) complexes derived from anti-inflammatory drugs show promise as multitarget colon cancer treatments. They inhibit key enzymes, modulate reactive oxygen species, and induce apoptosis while sparing healthy cells.

Area of Science:

  • Oncology
  • Medicinal Chemistry
  • Biochemistry

Background:

  • Targeting inflammation is a key strategy for cancer prevention and therapy.
  • Nonsteroidal anti-inflammatory drugs (NSAIDs) and metal-based drugs offer multitarget approaches against cancer progression.

Purpose of the Study:

  • To develop novel phosphane gold(I) complexes from NSAIDs as multitarget agents against colon cancer.
  • To investigate the antiproliferative mechanisms and selectivity of these gold complexes.

Main Methods:

  • Synthesis of new phosphane gold(I) complexes incorporating NSAIDs.
  • Evaluation of antiproliferative effects against colon cancer cells (Caco2-/TC7).
  • Assessment of mechanisms including cyclooxygenase inhibition, reactive oxygen species modulation (targeting thioredoxin reductase), and apoptosis induction.

Main Results:

  • Three complexes, [Au(L3)(JohnPhos)] (3b), [Au(L4)(CyJohnPhos)] (4a), and [Au(L4)(JohnPhos)] (4b), demonstrated significant antiproliferative activity.
  • Activity was linked to inhibition of cyclooxygenase-1/2, modulation of reactive oxygen species via thioredoxin reductase (TrxR) targeting, and apoptosis induction.
  • The active complexes showed high selectivity indices, sparing noncancerous cells.

Conclusions:

  • Phosphane gold(I) complexes derived from NSAIDs are effective multitarget agents against colon cancer.
  • These agents work by inhibiting key cancer-promoting enzymes and pathways.
  • Maintaining cellular redox balance and targeting TrxR are crucial for cancer cell survival and represent therapeutic opportunities.

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