Cytotoxic and cytostatic activity of copper(II) complexes. Importance of the speciation for the correct interpretation of the in vitro biological results

J Inorg Biochem. 1993 Apr 1;50(1):31-45. doi: 10.1016/0162-0134(93)80012-x.

Abstract

The cytotoxicity of some copper(II) compounds against the mouse cancer cell line B16, murine L929, human KB cells, and fibroblasts was investigated. All the copper(II) systems tested were shown to have pronounced toxicity against transformed cells and a cytostatic effect against untransformed cells, i.e., human fibroblasts. A careful speciation of the actual in vitro conditions reveals that copper(II) is essentially present as mixed complexes formed with the amino acids of the culture medium, [Cu(glutamine)(histidine)] being the main species. It was found that the cytotoxic activity is related to the amount of copper(II) contained in the tested compounds.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetates / chemistry
  • Acetates / pharmacology
  • Amino Acids
  • Animals
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use
  • Cell Death / drug effects
  • Cell Division / drug effects
  • Copper / chemistry*
  • Copper / pharmacology
  • Copper / therapeutic use
  • Fibroblasts / cytology
  • Fibroblasts / drug effects
  • Humans
  • Imidazoles / chemistry
  • Imidazoles / pharmacology
  • Melanoma, Experimental / drug therapy
  • Melanoma, Experimental / pathology
  • Mouth Neoplasms / drug therapy
  • Mouth Neoplasms / pathology
  • Tumor Cells, Cultured

Substances

  • Acetates
  • Amino Acids
  • Antineoplastic Agents
  • Imidazoles
  • Copper