4.7 Article

Enhanced concentration-dependent cytotoxic effect of the dinuclear copper(II) complex of L-carnitine [Cu2(L-carnitine)2Cl2(H2O)2]Cl2, compared to L-carnitine or copper chloride dihydrate, in human leukemic cell lines

Journal

JOURNAL OF MEDICINAL CHEMISTRY
Volume 51, Issue 13, Pages 3713-3719

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/jm701473x

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We studied the antitumor properties of the dinuclear copper(II) complex Of L-carnitine [Cu-2(L-carnitine)(2)Cl-2(H2O)(2)]Cl-2, as well as those Of L-carnitine and copper chloride dihydrate, in human leukemic cells. The complex was synthesized and characterized using EPR, H-1 NMR, C-13 NMR, IR, and UV- vis analyses. Its cytotoxic effect on the human leukemia cell lines HL-60 and K562 was studied by assessing the metabolic activity of cells (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide, MTT method), the structural integrity of cell membrane using Trypan blue assay, and the proliferation capacity of cells studying growth curves. Both leukemia cell lines showed a concentration-specific increased cytotoxicity of the complex, compared to L-carnitine or copper chloride dihydrate, with distinct underlying mechanisms, which were decreased proliferation efficiency for HL-60 cells and increased necrotic phenomena for K562 cells. Our results are indicative of a concentration-specific enhanced antileukemic effect of the complex, implying its value as a tool in the implementation of leukemia.

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