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Determination of Inhibition Efficiency of Carbamates Inhibitors of Acetylcholinesterase

Autoři: Vorčáková Katarína | Štěpánková Šárka | Zorič Petra | Štramová Xenie

Rok: 2013

Druh publikace: ostatní - přednáška nebo poster

Strana od-do: nestránkováno

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Jazyk	Název	Abstrakt	Klíčová slova
eng	Determination of Inhibition Efficiency of Carbamates Inhibitors of Acetylcholinesterase	Alzheimer´s disease is an age dependent neurodegenerative disorder that destroys brain cells, causes problems with memory, thinking and behaviour. There are many hypotheses of the etiology of this disease. The cholinergic hypothesis relates with increased activity of acetylcholinesterase (ACHE) and the neurodegeneration with the loss of cholinergic neurotransmission. ACHE is an enzyme primarily responsible for the rapid elimination of acetylcholine (ACH), within one millisecond after its release at cholinergic synapses. Nowadays, for treatment of AD inhibitors of ACHE are used. Ellman´s method (ELM) is based on measuring of yellow product which is formed in reaction between the thiol reagent 5,5?-dithiobis-2-nitrobenzoic acid and thiocholine (TCH), a product of substrate (acetylthiocholine, ATCH) hydrolysis by ACHE. Final concentration of ATCH in reaction mixture was 0.4 ?M. The electrochemical method is based on measuring of anodic oxidation current of TCH using square-wave voltammetry. Final concentration of ATCH in reaction mixture was 1 mM. The third one, pH-stat method is based on determination of actual concentration of acetic acid (HA) by continuous titration of HA with analytical solution of 0.1 M potassium hydroxide. Final concentration of ACH in reaction mixture was 1 mM. All measurements were carrying out with the final activity of ACHE in reaction mixture 0.2 U. For each measurement, the concentration of inhibitor was chosen experimentally so as to be visible inhibitory effect (slow hydrolysis). Inhibiting efficiency characterized by IC50 (concentration of inhibitor that causes a reduction of rate of inhibited reaction to one half compared to uninhibited reaction) was calculated. To the according data, the most effective inhibitor is 4-chlorobenzyl phenylcarbamate.	Carbamates; Inhibitors; Acetylcholinesterase

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