Selected ferrocenyl chalcones as DNA/BSA-interacting agents and inhibitors of DNA topoisomerase I and II activity

Eva Konkoľová, Jana Janočková, P. Perjési, Janka Vašková, Mária Kožurková

Research output: Contribution to journalArticle

2 Citations (Scopus)

Abstract

A series of four ferrocenyl chalcone derivatives (1-4) and one ferrocenyl non-chalcone derivative (5) were investigated with regards to their interactions with calf thymus DNA and bovine serum albumin (BSA). Study on the DNA/BSA interactive properties of complexes is one of the active subjects of bioorganic chemistry. It could provide fundamental data for developing potential therapeutic applications and understanding mechanism of action for drug. The interactions and binding characteristics of complexes with ctDNA and BSA were investigated using UV-Vis, CD and fluorescence spectroscopy. Moreover, topoisomerase inhibition assays were used to evaluate the ability of compounds to inhibit the activity of topoisomerases I/II. No interaction was detected between ctDNA and ferrocene derivatives. However, human topoisomerase I (hTOPI) was inhibited in a concentration-depend manner in the presence of compounds 1, 3, 4, although no inhibition was observed with compounds 2 and 5. In the case of human topoisomerase IIα, inhibition was observed and results indicate that these compounds can be classified as topoisomerase II suppressors, not poisons. The interaction between BSA and the four selected ligands (1-4) were studied by fluorescence quenching spectra. In addition, this method was used for the calculation of characteristic binding parameters. These results and results obtained by synchronous fluorescence spectra and 3D fluorescence spectra of the ferrocenyl chalcones with BSA determined that compounds create complexes with BSA and induce conformation changes.

Original languageEnglish
Pages (from-to)1-9
Number of pages9
JournalJournal of Organometallic Chemistry
Volume861
DOIs
Publication statusPublished - Apr 15 2018

Fingerprint

Chalcones
Topoisomerase I Inhibitors
Topoisomerase II Inhibitors
Bovine Serum Albumin
albumins
serums
inhibitors
DNA
deoxyribonucleic acid
Fluorescence
Derivatives
Type II DNA Topoisomerase
Thymus
fluorescence
Type I DNA Topoisomerase
Fluorescence spectroscopy
Conformations
Quenching
Assays
Ligands

Keywords

  • Bovine serum albumin
  • Calf thymus DNA
  • Ferrocenyl chalcones
  • Spectroscopic techniques
  • Topoisomerases I a II

ASJC Scopus subject areas

  • Biochemistry
  • Physical and Theoretical Chemistry
  • Organic Chemistry
  • Inorganic Chemistry
  • Materials Chemistry

Cite this

Selected ferrocenyl chalcones as DNA/BSA-interacting agents and inhibitors of DNA topoisomerase I and II activity. / Konkoľová, Eva; Janočková, Jana; Perjési, P.; Vašková, Janka; Kožurková, Mária.

In: Journal of Organometallic Chemistry, Vol. 861, 15.04.2018, p. 1-9.

Research output: Contribution to journalArticle

Konkoľová, Eva ; Janočková, Jana ; Perjési, P. ; Vašková, Janka ; Kožurková, Mária. / Selected ferrocenyl chalcones as DNA/BSA-interacting agents and inhibitors of DNA topoisomerase I and II activity. In: Journal of Organometallic Chemistry. 2018 ; Vol. 861. pp. 1-9.
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