Biological evaluation of a novel water soluble sulphur bridged binuclear copper(II) thiosemicarbazone complex

Eur J Med Chem. 2011 Sep;46(9):4584-94. doi: 10.1016/j.ejmech.2011.07.038. Epub 2011 Jul 28.

Abstract

The reaction of 2-oxo-1,2-dihydroquinoline-3-carbaldehyde 4(N,N)-dimethylthiosemicarbazone (HL) with copper(II) nitrate in methanol yielded water soluble [{Cu(L)(CH(3)OH)}(2)](NO(3))(2) · H(2)O. Structural analysis revealed that the complex consists of centrosymmetric binuclear entities containing square-pyramidal copper(II) ions bridged through the sulfur atoms. The spectroscopic experimental evidences strongly suggested that the ligand and complex could interact with calf thymus DNA (CT-DNA) through intercalation. A gel electrophoresis assay demonstrated the ability of the complex to cleave the pBR322 plasmid DNA. The complex also exhibited a strong binding to bovine serum albumin (BSA) over the ligand. Investigations of antioxidative properties showed that the complex has strong radical scavenging properties. Further, the cytotoxic effect of the complex was examined on HeLa, Hep G2, and HEp-2, which showed that the complex exhibited substantial cytotoxic specificity on HeLa over the other two.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cattle
  • Cell Line, Tumor
  • Crystallography, X-Ray
  • DNA / drug effects
  • Humans
  • Magnetic Resonance Spectroscopy
  • Models, Molecular
  • Solubility
  • Spectrometry, Fluorescence
  • Sulfur / chemistry*
  • Thiosemicarbazones / chemistry
  • Thiosemicarbazones / pharmacology*
  • Water

Substances

  • Thiosemicarbazones
  • Water
  • Sulfur
  • DNA