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Please use this identifier to cite or link to this item: http://hdl.handle.net/10651/10417

Title: Evaluation of antiproliferative activities and apoptosis induction caused by copper(II)-benzothiazolesulfonamide complexes in Jurkat T lymphocytes and Caco-2 cells
Author(s): González Álvarez, Marta
Alzuet Piña, Gloria
Borrás Tortonda, Joaquín
Castillo Agudo, Lucas del
Montejo Bernardo, José Manuel
Gutiérrez Rodríguez, Ángel
García-Granda, Santiago
Keywords: Copper(Ii)–Sulfonamide Complexes. Genotoxicity. Cell Proliferation Inhibition. Apoptosis
Issue date: 2008
Publisher version: http://dx.doi.org/10.1007/s00775-008-0409-0
Citation: Journal of Biological Inorganic Chemistry, 13(8), p. 1249-1265 (2008); doi:10.1007/s00775-008-0409-0
Format extent: p. 1249-1265
Abstract: Two copper(II) complexes with a benzothiazolesulfonamide ligand, [Cu(L)2(py)2] (1) and [Cu(en)2(L)2] (2) [HL is N-2-(4-methylbenzothiazole)toluenesulfonamide, py is pyridine, en is ethylenediamine], were prepared and then characterized with the aid of X-ray crystallography and spectroscopy. Whereas the copper(II) ion in 1 presents a square-planar geometry, in 2 it has a distorted octahedral environment. In addition, although the ligand is monodentate in both complexes, it exhibits different coordination behavior in each, interacting through the benzothiazole nitrogen atom in 1 and through the sulfonamide nitrogen atom in 2. The propensity for binding of 1 and 2 to calf thymus DNA was studied by thermal denaturation, viscosimetry, and cyclic voltammetry. The ability of the complexes to cleave DNA was studied in vitro through ascorbate activation and was tested by monitoring the expression of the yEGFP gene containing the RAD54 reporter. Moreover, their antiproliferative activity was verified in two cellular models: yeast and human tumor cells in culture. While 1 was found to be the more active cleaving agent in vitro, 2 showed a higher propensity for inflicting DNA damage at the cellular level. The biological studies carried out with human tumor cells, namely, colon adenocarcinoma Caco-2 cells (HTB-37) and leukemia Jurkat Tlymphocytes (TIB-152), confirmed that both compounds inhibit the growth of these cell lines, although 2 is more effective. This difference is associated with the latter compound’s greater ability to induce cell death by apoptosis.
URI: http://hdl.handle.net/10651/10417
ISSN: 0949-8257
Local identifier: 2538
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