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New gold carbene complexes as candidate anticancer agents.

Alessandro Pratesi1, Damiano Cirri1, Mirjana D Đurović2

  • 1(MetMed) Department of Chemistry, University of Florence, Via della Lastruccia 3, 50019, Sesto Fiorentino, Italy.

Biometals : an International Journal on the Role of Metal Ions in Biology, Biochemistry, and Medicine
|August 8, 2016
PubMed
Summary

Three gold(I) carbene complexes were evaluated as anticancer agents. Compound 1 showed higher activity against colon cancer cells, while all compounds were active against preosteoclast cells, suggesting potential therapeutic applications.

Keywords:
Anticancer drugsESI–MSGold carbeneProtein interaction

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Area of Science:

  • Medicinal Chemistry
  • Inorganic Chemistry
  • Cancer Biology

Background:

  • Gold(I) complexes are explored for anticancer properties.
  • Bulky hydrophobic ligands influence complex behavior and efficacy.
  • Understanding structure-activity relationships is crucial for drug development.

Purpose of the Study:

  • To investigate the anticancer potential of three novel gold(I) carbene complexes.
  • To compare the cytotoxic activity of these complexes against human colon cancer and preosteoclast cell lines.
  • To explore the interactions of these complexes with biomolecules like RNase A and glutathione.

Main Methods:

  • Synthesis and characterization of gold(I) carbene complexes 1-3.
  • In vitro cytotoxic assays using human colon cancer (HCT-116) and preosteoclast (FLG 29.1) cell lines.
  • Biochemical assays to study interactions with Ribonuclease A (RNase A) and glutathione (GSH).

Main Results:

  • Compound 1 exhibited significantly higher cytotoxicity against HCT-116 cells compared to compounds 2 and 3.
  • All three complexes demonstrated high and similar activity against FLG 29.1 cells.
  • Weak interactions were observed between complexes 1 and 2 with RNase A, forming minimal adducts.
  • Complex 2 showed reactivity towards GSH.

Conclusions:

  • The investigated gold(I) carbene complexes display differential cytotoxic activities, with compound 1 being particularly effective against colon cancer cells.
  • The complexes show promise as anticancer agents, especially for targeting preosteoclast cells.
  • Further studies are warranted to elucidate the precise mechanisms of action and optimize their therapeutic potential.