Crystal Structure, DNA Binding andCytotoxicity of a New Hydroxyl-Quinolinato Palladium Complex

The development of palladium anticancer drugs has been promising and their design has been basedmainly on the structure-activity relationship used for platinum anticancer drugs as well as good modelsfor the analogous Pt(II) complexes in solution[1-3].Thus our research in this area is focused on theinteraction of Calf Thymus DNA (CT-DNA)with a new palladium(II) anticancer complexof[Pd(8Q)(bpy)]NO3 (where 8Q = 8-hydroxyquinolin and bpy = 2, 2 -bipyridine).There is a set of 4binding sits(g) for the complex on the DNA with positive cooperativity in binding. n,the Hill coefficientfind out to be 5.25 at 300 and 4.36 at 310Krespectively. Kapp the apparent equilibrium constant are 45.58and 79.31 mM-1 respectively.The above compound can denature the DNA and the concentration of thisligand in the midpoint of transition ([L]1/2), is decreased by improving temperature, from 0.066 at 300to0.060 mmol/L at 310K. (ΔG0H2O) determined to be 31.64 and 25.19 kJ/mol at 300K and 310Krespectively. values for m, are 462.19and 381.51 at 300K and 310K respectively.ΔH0coformation in the rangeof 300K and 310K is find out to be 220.02 kJ/mol. ΔS0H2Oof DNA denaturation by complex is 0.627kJ/mol at 300K. Fluorescence titration spectra and fluorescence Scatchard plots suggest that the Pd(II)complex intercalate in DNA. The cytotoxicity assay of the complex has been performed on human breastadenocarcinoma MCF7 cell line, at micromolar concentration.

کلیدواژه ها:

Thermodinamic parameters ، spectroscopic techniques ، anti-tumor ، Palladium (II) complex