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Int. J. Mol. Sci. 2016, 17(9), 1560; doi:10.3390/ijms17091560

DNA Interaction Studies of Selected Polyamine Conjugates

1
Department of Hospital Pharmacy, Faculty of Pharmacy, Medical University of Lodz, 1 Muszynskiego Street, 90-151 Lodz, Poland
2
Food Science Department, Faculty of Pharmacy, Medical University of Lodz, 1 Muszynskiego Street, 90-151 Lodz, Poland
3
Department of Nucleic Acids Biochemistry, Medical University of Lodz, 251 Pomorska Street, 92-213 Lodz, Poland
4
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, Molecular and Cellular Biology)
View Full-Text   |   Download PDF [2281 KB, uploaded 19 September 2016]   |  

Abstract

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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MDPI and ACS Style

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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