Issue 9, 2016

Assessment of DNA-binding affinity of cholinesterase reactivators and electrophoretic determination of their effect on topoisomerase I and II activity

Abstract

In this paper, we describe the biochemical properties and biological activity of a series of cholinesterase reactivators (symmetrical bisquaternary xylene-linked compounds, K106–K114) with ctDNA. The interaction of the studied derivatives with ctDNA was investigated using UV-Vis, fluorescence, CD and LD spectrometry, and electrophoretic and viscometric methods. The binding constants K were estimated to be in the range 1.05 × 105–5.14 × 106 M−1 and the percentage of hypochromism was found to be 10.64–19.28% (from UV-Vis titration). The used methods indicate that the studied samples are groove binders. Electrophoretic methods proved that the studied compounds clearly influence calf thymus Topo I (at 5 μM concentration, except for compounds K107, K111 and K114 which were effective at higher concentrations) and human Topo II (K110 partially inhibited Topo II effects even at 5 μM concentration) activity.

Graphical abstract: Assessment of DNA-binding affinity of cholinesterase reactivators and electrophoretic determination of their effect on topoisomerase I and II activity

Supplementary files

Article information

Article type
Paper
Submitted
28 Apr. 2016
Accepted
06 Jūl. 2016
First published
06 Jūl. 2016

Mol. BioSyst., 2016,12, 2910-2920

Author version available

Assessment of DNA-binding affinity of cholinesterase reactivators and electrophoretic determination of their effect on topoisomerase I and II activity

J. Janockova, E. Zilecka, J. Kasparkova, V. Brabec, O. Soukup, K. Kuca and M. Kozurkova, Mol. BioSyst., 2016, 12, 2910 DOI: 10.1039/C6MB00332J

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