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Int. J. Mol. Sci. 2016, 17(9), 1560;

DNA Interaction Studies of Selected Polyamine Conjugates

Department of Hospital Pharmacy, Faculty of Pharmacy, Medical University of Lodz, 1 Muszynskiego Street, 90-151 Lodz, Poland
Food Science Department, Faculty of Pharmacy, Medical University of Lodz, 1 Muszynskiego Street, 90-151 Lodz, Poland
Department of Nucleic Acids Biochemistry, Medical University of Lodz, 251 Pomorska Street, 92-213 Lodz, Poland
Department of Medicinal Chemistry, Medical University of Lublin, 4 Jaczewskiego Street, 20-090 Lublin, Poland
Author to whom correspondence should be addressed.
Academic Editor: Mateus Webba da Silva
Received: 7 July 2016 / Revised: 9 September 2016 / Accepted: 9 September 2016 / Published: 19 September 2016
(This article belongs to the Section Biochemistry)
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The interaction of polyamine conjugates with DNA double helix has been studied. Binding properties were examined by ethidium bromide (EtBr) displacement and DNA unwinding/topoisomerase I/II (Topo I/II) activity assays, as well as dsDNA thermal stability studies and circular dichroism spectroscopy. Genotoxicity of the compounds was estimated by a comet assay. It has been shown that only compound 2a can interact with dsDNA via an intercalative binding mode as it displaced EtBr from the dsDNA-dye complex, with Kapp = 4.26 × 106 M−1; caused an increase in melting temperature; changed the circular dichroism spectrum of dsDNA; converted relaxed plasmid DNA into a supercoiled molecule in the presence of Topo I and reduced the amount of short oligonucleotide fragments in the comet tail. Furthermore, preliminary theoretical study has shown that interaction of the discussed compounds with dsDNA depends on molecule linker length and charge distribution over terminal aromatic chromophores. View Full-Text
Keywords: intercalation; polyamine conjugates; chromone; quinoline intercalation; polyamine conjugates; chromone; quinoline

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Szumilak, M.; Merecz, A.; Strek, M.; Stanczak, A.; Inglot, T.W.; Karwowski, B.T. DNA Interaction Studies of Selected Polyamine Conjugates. Int. J. Mol. Sci. 2016, 17, 1560.

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