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| rdf:type
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| rdfs:seeAlso
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| Description
| - This research was focused on a study of the binding properties of a series of cholinesterase reactivators compounds 1(075 (1), K027 (2) and inhibitors compounds 1(524, 1(009 and 7-MEOTA (3-5) with calf thymus DNA. The nature of the interactions between compounds 1-5 and DNA were studied using spectroscopic techniques (UV-vis, fluorescence spectroscopy and circular dichroism). The binding constants for complexes of cholinesterase modulators with DNA were determined from UV-vis spectroscopic titrations (K= 0.5 x 10(4)-8.9 x 10(5) M-1). The ability of the prepared analogues to relax topoisomerase I was studied with electrophoretic techniques and it was proved that ligands 4 and 5 inhibited this enzyme at a concentration of 30 mu.M. The biological activity of the novel compounds was assessed through an examination of changes in cell cycle distribution, mitochondrial membrane potential and cellular viability. Inhibitors 3-5 exhibited a cytotoxic effect on HL-60 (human acute promyelocytic leukaemia) cell culture, demonstrated a tendency to affect mitochondrial physiology and viability, and also forced cells to accumulate in the G(1) /G(0)-phase of the cell cycle. The cholinesterase reactivators 1 and 2 were found relatively save from the point of view of DNA binding, whereas cholinesterase inhibitors 3-5 resulted as strong DNA binding agents that limit their plausible use.
- This research was focused on a study of the binding properties of a series of cholinesterase reactivators compounds 1(075 (1), K027 (2) and inhibitors compounds 1(524, 1(009 and 7-MEOTA (3-5) with calf thymus DNA. The nature of the interactions between compounds 1-5 and DNA were studied using spectroscopic techniques (UV-vis, fluorescence spectroscopy and circular dichroism). The binding constants for complexes of cholinesterase modulators with DNA were determined from UV-vis spectroscopic titrations (K= 0.5 x 10(4)-8.9 x 10(5) M-1). The ability of the prepared analogues to relax topoisomerase I was studied with electrophoretic techniques and it was proved that ligands 4 and 5 inhibited this enzyme at a concentration of 30 mu.M. The biological activity of the novel compounds was assessed through an examination of changes in cell cycle distribution, mitochondrial membrane potential and cellular viability. Inhibitors 3-5 exhibited a cytotoxic effect on HL-60 (human acute promyelocytic leukaemia) cell culture, demonstrated a tendency to affect mitochondrial physiology and viability, and also forced cells to accumulate in the G(1) /G(0)-phase of the cell cycle. The cholinesterase reactivators 1 and 2 were found relatively save from the point of view of DNA binding, whereas cholinesterase inhibitors 3-5 resulted as strong DNA binding agents that limit their plausible use. (en)
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| Title
| - Interaction of cholinesterase modulators with DNA and their cytotoxic activity
- Interaction of cholinesterase modulators with DNA and their cytotoxic activity (en)
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| skos:prefLabel
| - Interaction of cholinesterase modulators with DNA and their cytotoxic activity
- Interaction of cholinesterase modulators with DNA and their cytotoxic activity (en)
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| skos:notation
| - RIV/62690094:18470/14:50002324!RIV15-MSM-18470___
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| http://linked.open...avai/riv/aktivita
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| http://linked.open...avai/riv/aktivity
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| http://linked.open...iv/cisloPeriodika
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| http://linked.open...vai/riv/dodaniDat
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| http://linked.open...aciTvurceVysledku
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| http://linked.open.../riv/druhVysledku
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| http://linked.open...iv/duvernostUdaju
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| http://linked.open...titaPredkladatele
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| http://linked.open...dnocenehoVysledku
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| http://linked.open...ai/riv/idVysledku
| - RIV/62690094:18470/14:50002324
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| http://linked.open...riv/jazykVysledku
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| http://linked.open.../riv/klicovaSlova
| - Cytotoxicity; HL-60; Topoisomerase I; DNA; Oximes; Cholinesterase modulators (en)
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| http://linked.open.../riv/klicoveSlovo
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| http://linked.open...odStatuVydavatele
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| http://linked.open...ontrolniKodProRIV
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| http://linked.open...i/riv/nazevZdroje
| - International journal of biological macromolecules
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| http://linked.open...in/vavai/riv/obor
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| http://linked.open...ichTvurcuVysledku
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| http://linked.open...cetTvurcuVysledku
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| http://linked.open...UplatneniVysledku
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| http://linked.open...v/svazekPeriodika
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| http://linked.open...iv/tvurceVysledku
| - Kuča, Kamil
- Musílek, Kamil
- Mikeš, Jaromír
- Culka, Lubomír
- Fedorocko, Peter
- Gulášová, Zuzana
- Janočková, Jana
- Kozurková, Maria
- Plšíková, Jana
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| http://linked.open...ain/vavai/riv/wos
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| issn
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| number of pages
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| http://bibframe.org/vocab/doi
| - 10.1016/j.ijbiomac.2013.11.022
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| http://localhost/t...ganizacniJednotka
| |
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