alexa Spectroscopic Studies of the Bis-3,6-Alkylamidoacridines as Potential Topoisomerase I Inhibitors | OMICS International | Abstract
ISSN: 2168-9652

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Research Article

Spectroscopic Studies of the Bis-3,6-Alkylamidoacridines as Potential Topoisomerase I Inhibitors

Danica Sabolová1*, Júlia Kudláčová1, Ladislav Janovec2 and Ján Imrich2
1Faculty of Science, Department of Biochemistry, Institute of Chemistry, P.J. Šafárik University, Slovak Republic
2Department of Organic Chemistry, Institute of Chemistry, P.J. Šafárik University, Slovak Republic
*Corresponding Author : Danica Sabolová
Faculty of Science, Department of Biochemistry
Institute of Chemistry, P.J. Šafárik University
Moyzesova 11, 04167 Košice, Slovak Republic
Tel: 421 55 6223582
E-mail: [email protected]
Received June 26, 2013; Accepted July 16, 2013; Published July 19, 2013
Citation: Sabolová D, Kudlácová J, Janovec L, Imrich J (2013) Spectroscopic Studies of the Bis-3,6-Alkylamidoacridines as Potential Topoisomerase I Inhibitors. Biochem Physiol 2:112. doi:10.4172/2168-9652.1000112
Copyright: © 2013 Sabolová D, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.

Abstract

In this paper, the interaction of bis-3,6-alkylamidoacridines with calf thymus DNA (ctDNA) and their inhibitory effect on topoisomerase I are investigated. The binding mode of the low-molecular ligands to ctDNA was determined using UVvis absorption spectrophotometry, fluorescence spectrophotometry and circular dichroism. The binding constants for the DNA-drug complexes were estimated to be from 2.10×105 to 0.68×105 M-1, and the percentage of hypochromism was found to be over 25% (from UV-vis titrations). The effect of the investigated compounds on the transition temperature of ctDNA was detected using thermal denaturation studies. Experiments using arose gel electrophoresis demonstrated that the tested derivatives have an inhibitory effect on topoisomerase I.

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