title: DNA Interaction Studies of Selected Polyamine Conjugates.
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 compound2acan interact with dsDNA via an intercalative binding mode as it displaced EtBr from the dsDNA-dye complex, withKapp= 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.
authors.affiliation: Department of Hospital Pharmacy, Faculty of Pharmacy, Medical University of Lodz, 1 Muszynskiego Street, 90-151 Lodz, Poland. marta.szumilak@umed.lodz.pl.
authors.forename: Marta
authors.initials: M
authors.lastname: Szumilak
authors.affiliation: Food Science Department, Faculty of Pharmacy, Medical University of Lodz, 1 Muszynskiego Street, 90-151 Lodz, Poland. anna.merecz@umed.lodz.pl.
authors.forename: Anna
authors.initials: A
authors.lastname: Merecz
authors.affiliation: Department of Nucleic Acids Biochemistry, Medical University of Lodz, 251 Pomorska Street, 92-213 Lodz, Poland. malgorzata.strek@umed.lodz.pl.
authors.forename: Malgorzata
authors.initials: M
authors.lastname: Strek
authors.affiliation: Department of Hospital Pharmacy, Faculty of Pharmacy, Medical University of Lodz, 1 Muszynskiego Street, 90-151 Lodz, Poland. andrzej.stanczak@umed.lodz.pl.
authors.forename: Andrzej
authors.initials: A
authors.lastname: Stanczak
authors.affiliation: Department of Medicinal Chemistry, Medical University of Lublin, 4 Jaczewskiego Street, 20-090 Lublin, Poland. tadeusz.inglot@umlub.pl.
authors.forename: Tadeusz W
authors.initials: TW
authors.lastname: Inglot
authors.affiliation: Food Science Department, Faculty of Pharmacy, Medical University of Lodz, 1 Muszynskiego Street, 90-151 Lodz, Poland. boleslaw.karwowski@umed.lodz.pl.
authors.forename: Boleslaw T
authors.initials: BT
authors.lastname: Karwowski
keywords: chromone; intercalation; polyamine conjugates; quinoline