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Published on: March 18, 2015

Thioredoxin reductase and cancer cell growth inhibition by organogold(III) compounds

Lars Engman1, Michael McNaughton, Malgorzata Gajewska

  • 1Organic Chemistry, Department of Chemistry, Uppsala University, Uppsala, Sweden. Lars.Engman@kemi.uu.se

Anti-Cancer Drugs
|May 17, 2006
PubMed

Insights

Gold(III) compounds show potential for cancer therapy by inhibiting thioredoxin reductase (TrxR). However, their effectiveness in killing cancer cells and in vivo anti-tumor activity requires further investigation.

Area of Science:

  • Medicinal Chemistry
  • Cancer Biology
  • Organometallic Chemistry

Background:

  • Thioredoxin (Trx) system is upregulated in many cancers, promoting tumor growth and reducing survival.
  • The Trx/Trx reductase (TrxR) system is a promising target for novel anti-cancer drug development.

Purpose of the Study:

  • To evaluate gold(III) compounds with varying carbon-gold bonds for TrxR inhibition and anti-cancer activity.
  • To assess the correlation between TrxR inhibition and cancer cell growth inhibition.

Main Methods:

  • Synthesis and evaluation of various gold(III) compounds.
  • In vitro assays for TrxR inhibition (IC50 values).
  • In vitro cancer cell growth inhibition assays (MCF-7 cells).
  • In vivo studies using xenografts (MCF-7 and HT-29) in scid mice.

Main Results:

  • Gold(III) compounds with up to two carbon-gold bonds potently inhibited TrxR (IC50 as low as 2 nmol/l).
  • TrxR inhibition was reduced in the presence of Trx and insulin.
  • Inhibitory concentrations for TrxR did not correlate with cancer cell killing efficacy.
  • Compound 8 (two carbon-gold bonds) inhibited MCF-7 colony formation (IC50=1.6 micromol/l) but lacked in vivo anti-tumor activity.

Conclusions:

  • Gold(III) compounds can effectively inhibit TrxR, but this does not directly translate to potent anti-cancer effects in vitro or in vivo.
  • Further research is needed to develop gold-based drugs that overcome limitations in cancer cell killing and in vivo efficacy.

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