Application of Human Cholinesterase in Determination of Inhibitory Effect of Salicylanilide diethyl phosphates

Kód výsledku v IS VaVaI

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Výsledek na webu

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DOI - Digital Object Identifier

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Jazyk výsledku

angličtina

Název v původním jazyce

Application of Human Cholinesterase in Determination of Inhibitory Effect of Salicylanilide diethyl phosphates

Popis výsledku v původním jazyce

The aim of our study was in vitro determination of inhibitory effect of ten substituted salicylanilide diethyl phosphates to both of human cholinesterases. The source of enzymes was the blood which was obtained from volunteer donors. Inhibition efficiency of tested inhibitors was described by the value of IC50 (50% inhibiting concentration). Final activity of human enzymes was calculated for used reaction conditions. The concentration of substrate (acetylthiocholine and butyrylthiocholine) was 1.10-3 M.All tested inhibitors are potent inhibitors of human cholinesterases. Compound 8 ((O-{4-bromo-2-[(3,4-dichlorophenyl)carbamoyl]phenyl} O,O-diethyl thiophosphate) was the most effective inhibitor of HuAChE and the compound 3 (O-{4-chloro-2-[(4-chlorophenyl)carbamoyl]phenyl} O,O-diethyl thiophosphate) was the most effective inhibitor of HuBChE for both of used substrates.

Název v anglickém jazyce

Application of Human Cholinesterase in Determination of Inhibitory Effect of Salicylanilide diethyl phosphates

Popis výsledku anglicky

The aim of our study was in vitro determination of inhibitory effect of ten substituted salicylanilide diethyl phosphates to both of human cholinesterases. The source of enzymes was the blood which was obtained from volunteer donors. Inhibition efficiency of tested inhibitors was described by the value of IC50 (50% inhibiting concentration). Final activity of human enzymes was calculated for used reaction conditions. The concentration of substrate (acetylthiocholine and butyrylthiocholine) was 1.10-3 M.All tested inhibitors are potent inhibitors of human cholinesterases. Compound 8 ((O-{4-bromo-2-[(3,4-dichlorophenyl)carbamoyl]phenyl} O,O-diethyl thiophosphate) was the most effective inhibitor of HuAChE and the compound 3 (O-{4-chloro-2-[(4-chlorophenyl)carbamoyl]phenyl} O,O-diethyl thiophosphate) was the most effective inhibitor of HuBChE for both of used substrates.

Druh

D - Stať ve sborníku

CEP obor

CE - Biochemie

OECD FORD obor

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Projekt

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Návaznosti

S - Specificky vyzkum na vysokych skolach

Rok uplatnění

2015

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název statě ve sborníku

4th International Miniconference of PhD Students: When Biochemistry Meets Pharmacology and Toxicology

ISBN

978-80-971042-5-2

ISSN

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e-ISSN

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Počet stran výsledku

4

Strana od-do

17-20

Název nakladatele

Ústav experimentálnej farmakológie a toxikológie SAV

Místo vydání

Bratislava

Místo konání akce

Bratislava

Datum konání akce

24. 6. 2015

Typ akce podle státní příslušnosti

EUR - Evropská akce

Kód UT WoS článku

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