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Mol Biosyst ; 12(9): 2910-20, 2016 08 16.
Artículo en Inglés | MEDLINE | ID: mdl-27412811

RESUMEN

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 × 10(5)-5.14 × 10(6) 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.


Asunto(s)
Reactivadores de la Colinesterasa/química , ADN-Topoisomerasas de Tipo II/química , ADN-Topoisomerasas de Tipo I/química , ADN/química , Reactivadores de la Colinesterasa/farmacología , Dicroismo Circular , ADN/metabolismo , ADN-Topoisomerasas de Tipo I/metabolismo , ADN-Topoisomerasas de Tipo II/metabolismo , Estructura Molecular , Desnaturalización de Ácido Nucleico , Unión Proteica , Análisis Espectral , Viscosidad
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