Abstract
The two water-soluble designed platinum(II) complex, [Pt(Oct-dtc)(bpy)]NO3 (Oct-dtc = Octyldithiocarbamate and bpy = 2,2′ -bipyridine) and palladium(II) complex, [Pd(Oct-dtc)(bpy)]NO3, have been synthesized and characterized by elemental analyses, molar conductivity measurements, IR, 1H NMR, and electronic spectra studies. Studies of antitumor activity of these complexes against human cell tumor lines (K562) have been carried out. They show Ic50 values lower than that of cisplatin. The complexes have been investigated for their interaction with calf thymus DNA (CT-DNA) by utilizing the electronic absorption spectroscopy, fluorescence spectra, and ethidium bromide displacement and gel filtration techniques. Both of these water-soluble complexes bound cooperatively and intercalatively to the CT-DNA at very low concentrations. Several binding and thermodynamic parameters are also described.
Highlights
In order to reduce the toxicity of cisplatin, that is, the wellknown anticancer drug, and modulate its activity, a new strategy is the design of novel metal complexes containing N and S donor ligands [1,2,3]
Cytotoxic Measurement of the Metal Complexes. [Pt/Pd(Oct-dtc)]NO3 complexes were screened for their antitumor activities against K562 chronic myelogenous leukemia cells [15]
The harvested cells were seeded into 96-well plate (1 × 104 cell/mL) with various concentrations of metal complexes ranging from 0 to 0.25 mM and incubated for 24 h [42]
Summary
In order to reduce the toxicity of cisplatin, that is, the wellknown anticancer drug, and modulate its activity, a new strategy is the design of novel metal complexes containing N and S donor ligands [1,2,3]. This interest has probably initiated from detoxicant properties of sulfur-containing ligands against heavy metal intoxication [4]. Diethyldithiocarbamate has remarkable property of reversing platinum binding to macromolecules responsible for host toxicity. The protective action of the dithiocarbamate against the toxicity of cisplatin seems to be the formation of its stable platinum dithiocarbamate complexes [7, 10]
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