Interaction of cholinesterase modulators with DNA and their cytotoxic activity
Identifikátory výsledku
Kód výsledku v IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00179906%3A_____%2F14%3A10209873" target="_blank" >RIV/00179906:_____/14:10209873 - isvavai.cz</a>
Nalezeny alternativní kódy
RIV/62690094:18470/14:50002324
Výsledek na webu
<a href="http://www.sciencedirect.com/science/article/pii/S0141813013006314" target="_blank" >http://www.sciencedirect.com/science/article/pii/S0141813013006314</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1016/j.ijbiomac.2013.11.022" target="_blank" >10.1016/j.ijbiomac.2013.11.022</a>
Alternativní jazyky
Jazyk výsledku
angličtina
Název v původním jazyce
Interaction of cholinesterase modulators with DNA and their cytotoxic activity
Popis výsledku v původním jazyce
This research was focused on a study of the binding properties of a series of cholinesterase reactiva-tors compounds K075 (1), K027 (2) and inhibitors compounds K524, K009 and 7-MEOTA (3-5) with calfthymus DNA. The nature of the interactions between compounds 1-5 and DNA were studied using spec-troscopic techniques (UV-vis, fluorescence spectroscopy and circular dichroism). The binding constantsfor complexes of cholinesterase modulators with DNA were determined from UV-vis spectroscopic titra-tions (K =0.5 x 104-8.9 x 105MMINUS SIGN 1). The ability of the prepared analogues to relax topoisomerase I wasstudied with electrophoretic techniques and it was proved that ligands 4 and 5 inhibited this enzymeat a concentration of 30 M. The biological activityof the novel compounds was assessed through anexamination of changes in cell cycle distribution, mitochondrial membrane potential and cellular via-bility. Inhibitors 3-5 exhibited a cytotoxic effect on HL-60 (human acute promyelocytic leu
Název v anglickém jazyce
Interaction of cholinesterase modulators with DNA and their cytotoxic activity
Popis výsledku anglicky
This research was focused on a study of the binding properties of a series of cholinesterase reactiva-tors compounds K075 (1), K027 (2) and inhibitors compounds K524, K009 and 7-MEOTA (3-5) with calfthymus DNA. The nature of the interactions between compounds 1-5 and DNA were studied using spec-troscopic techniques (UV-vis, fluorescence spectroscopy and circular dichroism). The binding constantsfor complexes of cholinesterase modulators with DNA were determined from UV-vis spectroscopic titra-tions (K =0.5 x 104-8.9 x 105MMINUS SIGN 1). The ability of the prepared analogues to relax topoisomerase I wasstudied with electrophoretic techniques and it was proved that ligands 4 and 5 inhibited this enzymeat a concentration of 30 M. The biological activityof the novel compounds was assessed through anexamination of changes in cell cycle distribution, mitochondrial membrane potential and cellular via-bility. Inhibitors 3-5 exhibited a cytotoxic effect on HL-60 (human acute promyelocytic leu
Klasifikace
Druh
J<sub>x</sub> - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)
CEP obor
FR - Farmakologie a lékárnická chemie
OECD FORD obor
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Návaznosti výsledku
Projekt
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Návaznosti
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
Ostatní
Rok uplatnění
2014
Kód důvěrnosti údajů
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Údaje specifické pro druh výsledku
Název periodika
International Journal of Biological Macromolecules
ISSN
0141-8130
e-ISSN
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Svazek periodika
64
Číslo periodika v rámci svazku
March
Stát vydavatele periodika
NL - Nizozemsko
Počet stran výsledku
10
Strana od-do
53-62
Kód UT WoS článku
000334147300009
EID výsledku v databázi Scopus
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