Abstract
Indole-2-carboxylic acid copper complex (ICA-Cu) was successfully prepared and characterized through elemental analysis, IR, UV-Vis, 1H-NMR, TG analysis, and molar conductance, and its molecular formula was [Cu2(C9H6O2N)4(H2O)2]·2H2O. The binding ability of ICA-Cu to calf thymus DNA (CT-DNA) was examined by fluorescence spectrometry and the viscosity method. The results indicated that, upon the addition of increasing amounts of CT-DNA, the excitation and emission intensity of ICA-Cu decreased obviously and the excitation spectra shifted towards a long wavelength. ICA-Cu could displace ethidium bromide (EB) from the EB-DNA system, making the fluorescence intensity of the EB-DNA system decrease sharply; the quenching constant KSV value was 3.99 × 104 M−1. The emission intensity of the ICA-Cu-DNA system was nearly constant, along with the addition of Na+ in a series of concentrations. The fluorescence of the complex could be protected after the complex interacted with DNA. A viscosity measurement further supported the result that the ICA-Cu complex may interact with DNA in an intercalative binding mode. The antioxidant activities of ICA-Cu were evaluated by a 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay, a hydroxyl radical (OH) scavenging assay, and a 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid (ABTS) assay. The ICA-Cu exhibited the highest inhibitory effects on the ABTS radical (94% inhibition at 60 µM), followed by OH and DPPH radicals (the degrees of inhibition being 71% and 56%, respectively). The in vitro cytotoxicity activity of ICA-Cu against two human breast cancer cell lines, MDA-MB-231 and MCF-7, was investigated by 3-[4,5-dimethyltiazol2-yl]-2.5-diphenyl-tetrazolium bromide (MTT) assay and cellular morphological analysis. The results showed that, upon increasing the concentration of ICA-Cu, an increase was observed in growth-inhibitory activity and the inhibition percentage were greater than 90% at 20 µM in both cell lines. Also, cellular morphological changes in the two cell lines agreed with the cytotoxicity results.
Highlights
Cancer has become the leading cause of death of the world, since the incidence of cancer is increasing every year [1,2]
The binding ability of the complex to CT-DNA was studied by fluorescence spectrometry and the viscosity method, and we found that indole-2-carboxylic acid (ICA)-Cu possibly binds to to DNA
We previously demonstrated that indole-3-carboxylic acid metal complexes exhibit potent anticancer activity on breast and prostate cancer cells
Summary
Cancer has become the leading cause of death of the world, since the incidence of cancer is increasing every year [1,2]. Current studies have demonstrated that a number of metal-based as complexes copper, manganese, possess promising inhibitory activities on various cancer andcancer have been of gold, and gallium, copper, and manganese, possess promising inhibitory activities on cells various cells evaluated in vitro and in vivo in cancer therapy and Cattaruzza etand al. Has exhibited with the inhibition of More proteasome recently, we have studied a new potent antiproliferative activity onantiproliferative human breast cancer cells. The complex could inhibit complex that has exhibited potent activity on human breast cancer cells. (DDTC)-Cu, and(PDTC)-Cu, some Schiffdiethyldithiocarbamate base Cu complexes, were found to and possess potent activities were found possess potent antitumor activities in vitro or in vivo [19,20,21,22,23]. Chemical structure of the Indole-2-carboxylic acid copper complex (ICA-Cu)
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