Research Article
Spectroscopic Studies of the Bis-3,6-Alkylamidoacridines as Potential Topoisomerase I Inhibitors
| Danica Sabolová1*, Júlia Kudlá脙鈥灻偮峯vá1, 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: danica.sabolova@upjs.sk |
| 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.
