BIAN N-Heterocyclic Gold Carbene Complexes induced cytotoxicity in human cancer cells via upregulating oxidative stress

Asian Pac J Cancer Prev. 2015;16(16):7003-6. doi: 10.7314/apjcp.2015.16.16.7003.

Abstract

Background: Nanoparticles of gold and silver are offering revolutionary changes in the field of cancer therapy. N-heterocyclic carbene (NHC) metal complexes possess diverse biological activities and are being investigated as potential chemotherapeutic agents. The purpose of this study was to examine the cytotoxicity and possible mechanisms of action of two types of newly synthesized nanofiber composites containing BIAN N-heterocyclic gold carbene complexes in two types of human cancer cells, namely breast cancer (MCF7) and liver cancer (HepG2) cells and also in normal human embryonic kidney cells (HEK 293).

Materials and methods: Cytotoxicity was assessed by MTT cell viability assay and oxidative stress by checking the total glutathione level.

Results: Both compounds affected the cell survival of the tested cell lines at very low concentrations (IC50 values in the micro molar range) as compared to a well-known anti-cancer drug, 5 fluorouracil. A 60-80% depletion in total glutathione level was detected in treated cells.

Conclusions: Reduction in total glutathione level is one of the biochemical pathways for the induction of oxidative stress which in turn could be a possible mechanism of action by which these compounds induce cytotoxicity in cancer cell lines. The in vitro toxicity towards cancer cells found here means that these molecules could be potential anticancer candidates.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acenaphthenes / pharmacology*
  • Antineoplastic Agents / pharmacology*
  • Cell Survival / drug effects
  • Coordination Complexes / pharmacology
  • Fluorouracil / pharmacology
  • Glutathione / metabolism
  • Gold / pharmacology*
  • HEK293 Cells
  • Hep G2 Cells
  • Heterocyclic Compounds / pharmacology*
  • Humans
  • Inhibitory Concentration 50
  • MCF-7 Cells
  • Methane / analogs & derivatives*
  • Methane / pharmacology
  • Nanofibers
  • Oxidative Stress / drug effects*

Substances

  • Acenaphthenes
  • Antineoplastic Agents
  • Coordination Complexes
  • Heterocyclic Compounds
  • carbene
  • Gold
  • Glutathione
  • Methane
  • Fluorouracil