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Application of Human Cholinesterase in Determination of Inhibitory Effect of Salicylanilide diethyl phosphates
Authors: Vorčáková Katarína | Štěpánková Šárka | Krátky Martin | Vinšová Jarmila
Year: 2015
Type of publication: článek ve sborníku
Name of source: 4th International Miniconference of PhD Students: When Biochemistry Meets Pharmacology and Toxicology
Publisher name: Ústav experimentálnej farmakológie a toxikológie SAV
Place: Bratislava
Page from-to: 17-20
Titles:
Language Name Abstract Keywords
cze Stanovení inhibičního efektu salicylanilid dietylfosfátov na lidské cholinesterázy Cílem práce bylo in vitro testování deseti salicylanilid dietylfosfátů na lidské cholinesterázy. Zdrojem enzymu byla lidská krev dobrovolných dárců. V prvním kroku byla vypočítaná aktuální aktivita lidských enzymů a následně byla stanovená 50% inhibiční koncentrace. Všechny testované sloučeniny vykazovali inhibiční účinek na lidské cholinesterázy. lidské cholinesterázy; IC50; salicylanilid dietylfosfáty; Ellmanová metoda
eng Application of Human Cholinesterase in Determination of Inhibitory Effect of Salicylanilide diethyl phosphates 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. human cholinesterases; IC50; salicylanilide diethyl phosphates; Ellman's method

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