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Antimicrobial activity and DNA/HSA interaction of fluorinated 3,6,9-trisubstituted acridines

Authors
  • Nunhart, Patrik1
  • Konkoľová, Eva1
  • Janovec, Ladislav1
  • Kašpárková, Jana2
  • Malina, Jaroslav2
  • Brabec, Viktor2
  • Matejová, Mária1
  • Miltáková, Beata1
  • Novotny, Ladislav3
  • Phillips, Oludotun A.3
  • Udo, Edet3
  • Kozurkova, Mária1, 4
  • 1 P. J. Šafárik University in Košice, Šrobárova 2, Košice, 041 54, Slovak Republic , Košice (Slovakia)
  • 2 Palacky University in Olomouc, Olomouc, Czech Republic , Olomouc (Czechia)
  • 3 Kuwait University, Kuwait City, Kuwait , Kuwait City (Kuwait)
  • 4 University Hospital Hradec Kralove, Sokolovska 581, Hradec Kralove, 500 05, Czech Republic , Hradec Kralove (Czechia)
Type
Published Article
Journal
Chemical Papers
Publisher
Springer International Publishing
Publication Date
Feb 03, 2020
Volume
74
Issue
7
Pages
2327–2337
Identifiers
DOI: 10.1007/s11696-020-01079-4
Source
Springer Nature
Keywords
License
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Abstract

A series of four new 3,6,9-trisubstituted acridine derivatives (two with fluorine substituents on phenyl ring) were synthesized and their interaction with calf thymus DNA and HSA was investigated using a combination of biochemical, biophysical and biological techniques. Analysis using fluorescent spectra provided valuable information about the formation of the acridine–DNA complex, while several other experiments suggest that acridine may bind to DNA through intercalation. These observations are further supported by LD spectral analysis, viscosity measurements and DNA melting studies. The interaction between HSA and four compounds were studied by fluorescence quenching spectra. In addition, the method was used for the calculation of characteristic binding parameters. These result and result obtained by synchronous fluorescence spectra of acridines with HSA determined that compounds create complexes with HSA and induce conformational changes. KB values were found to be of 1.51–7.34 × 106 M−1. The studied 8c compound were the most sensitive against S. epidermidis ATCC 12228.

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