4.7 Article

Synthesis, cellular uptake, apopotosis, cytotoxicity, cell cycle arrest, interaction with DNA and antioxidant activity of ruthenium(II) complexes

Journal

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 46, Issue 8, Pages 3282-3290

Publisher

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2011.04.049

Keywords

Ruthenium(II) complexes; Cytotoxicity; Apoptosis; Cellular uptake; DNA-binding

Funding

  1. National Nature Science Foundation of China [30800227, 31070858]
  2. Guangdong Pharmaceutical University

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A new ligand and two ruthenium(II) complexes [Ru(bpy)(2)(DNPIP)](ClO4)(2) 1 and [Ru(bpy)(2)(DAPIP)](ClO4)(2) 2 were synthesized and characterized. The DNA-binding constants for complexes 1 and 2 were determined to be 2.24 (+/-0.30) x 10(5) M-1 (s = 1.29) and 6.34 (+/-0.32) x 10(4) M-1 (s = 2.84). The photocleavage of pBR322 DNA by Ru(II) complexes was investigated. The cytotoxicity of complexes 1 and 2 were assessed against three tumor cell lines. The apoptosis and cellular uptake were studied. The retardation assay of pGL 3 plasmid DNA was explored. The cell cycle arrest was analysized by flow cytometry. The antioxidant activities of the ligand and complexes were also investigated. Crown Copyright (C) 2011 Published by Elsevier Masson SAS. All rights reserved.

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