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


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).


CONCLUSIONS
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.
Van Rensburg
Constance E J
CE
Department of Immunology, Institute for Pathology, University of Pretoria, South Africa.
Kreft
Elke
E
Swarts
Jannie C
JC
Dalrymple
Sean R
SR
MacDonald
Denise M
DM
Cooke
Michael W
MW
Aquino
Manuel A S
MA
D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000633:toxicity*; D004354:Drug Screening Assays, Antitumor; D006367:HeLa Cells / Q000187:drug effects; D006801:Humans; D007941:Leukemia P388 / Q000188:drug therapy; D051379:Mice; D009942:Organometallic Compounds / Q000737:chemistry / Q000633:toxicity*; D012428:Ruthenium / Q000737:chemistry / Q000633:toxicity*
D000970:Antineoplastic Agents; D009942:Organometallic Compounds; D012428:Ruthenium