Cytotoxicity, apoptosis, cellular uptake, cell cycle arrest, photocleavage, and antioxidant activity of 1, 10-phenanthroline ruthenium(II) complexes

DNA Cell Biol. 2011 Oct;30(10):839-48. doi: 10.1089/dna.2011.1243. Epub 2011 May 13.

Abstract

Two new ruthenium(II) complexes, [Ru(phen)2(DNPIP)](ClO4)2 (1) and [Ru(phen)2(DAPIP)](ClO4)2 (2), were synthesized and characterized. The DNA-binding properties of these complexes were investigated using UV/vis absorption titration, viscosity measurements, thermal denaturation, and photoactivated cleavage. The DNA binding constants for complexes 1 and 2 are 2.63 ± 0.25×10(5) M(-1) (s=2.45) and 1.51±0.18×10(5) M(-1) (s=1.34). The results indicated that these complexes interacted with DNA through the intercalative mode. The cytotoxicity in vitro of complexes 1 and 2 were assessed against BEL-7402, HepG-2, and MCF-7 cell lines by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Apoptosis was studied with the acridine orange/ethidium bromide staining method. The antiproliferative mechanism was explored with flow cytometry. Cellular uptake studies showed that complexes 1 and 2 can enter into the cytoplasm and accumulate in the nuclei. Cell cycle arrest and antioxidant activity were also investigated.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / pharmacology*
  • Antioxidants / chemical synthesis
  • Antioxidants / pharmacology*
  • Apoptosis / drug effects
  • Breast Neoplasms / drug therapy
  • Breast Neoplasms / pathology
  • Cell Line, Tumor
  • Cell Nucleus / metabolism
  • Cell Survival / drug effects
  • Cell Survival / radiation effects
  • DNA / chemistry
  • DNA / metabolism*
  • Electrophoretic Mobility Shift Assay
  • Female
  • Flow Cytometry
  • Fluorescence
  • Humans
  • Hydroxyl Radical / antagonists & inhibitors
  • Hydroxyl Radical / metabolism
  • Intercalating Agents / chemical synthesis
  • Intercalating Agents / pharmacology*
  • Kinetics
  • Liver Neoplasms / drug therapy
  • Liver Neoplasms / pathology
  • Organometallic Compounds / chemical synthesis
  • Organometallic Compounds / pharmacology*
  • Oxidation-Reduction / drug effects
  • Oxidation-Reduction / radiation effects
  • Phenanthrolines / chemistry
  • Photolysis / radiation effects
  • Plasmids / metabolism
  • Ruthenium / chemistry
  • Ruthenium / metabolism*
  • Spectrum Analysis
  • Ultraviolet Rays

Substances

  • Antineoplastic Agents
  • Antioxidants
  • Intercalating Agents
  • Organometallic Compounds
  • Phenanthrolines
  • Hydroxyl Radical
  • Ruthenium
  • DNA
  • calf thymus DNA