Cytotoxicity of a series of water-soluble mixed valent diruthenium tetracarboxylates.

Abstract

BACKGROUND:

Mixed-valent diruthenium tetracarboxylate complexes were shown to have slight antineoplastic activity against P388 leukemia cell lines. However these complexes suffered from poor water-solubility, which may have detrimentally affected their activity.

MATERIALS AND METHODS:

Mixed-valent diruthenium tetracarboxylates of the type [Ru2(O2CR)4(L)2] (PF6) with L = imidazole, 1-methylimidazole and H2O when R = CH3, L = ethanol when R = Fc (ferrocenyl) or Fc-CH=CH- and of the type M3[Ru2(O2CR)4(H2O)2]4H2O, M = Na+ when R = m-C6H4SO3- and M = K+ when R = p-C6H4SO3-, were tested for cytotoxicity against HeLa and multidrug resistant CoLo 320DM human cancer cell lines. Cell survival was measured by means of the colorometric 3-(4,5dimethylthiazol-2-yl)-diphenyltetrazodium bromide assay.

RESULTS:

The mean drug concentration from 3 experiments causing 50% cell killing, ie, IC50 values, varied between 120 and 950 micromol dm(-3).

CONCLUSION:

The antineoplastic activity of the highly water-soluble m-sulpho derivative was the highest, while the poorly water-soluble imidazole derivatives did not exhibit any cytotoxic properties. The CoLo 320DM cancer cells were 5 times more prone to drug-induced cell death than the HeLa cells.

• Authors: Constance E J Van Rensburg, Elke Kreft, Jannie C Swarts, Sean R Dalrymple, Denise M MacDonald, Michael W Cooke, Manuel A S Aquino
• Journal: Anticancer research (Anticancer Res) 2002 Mar-Apr Vol. 22 Issue 2A Pg. 889-92 ISSN: 0250-7005 [Print] Greece
• PMID: 12014667 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antineoplastic Agents
• Organometallic Compounds
• Ruthenium

Topics

• Animals
• Antineoplastic Agents (chemistry, toxicity)
• Drug Screening Assays, Antitumor
• HeLa Cells (drug effects)
• Humans
• Leukemia P388 (drug therapy)
• Mice
• Organometallic Compounds (chemistry, toxicity)
• Ruthenium (chemistry, toxicity)