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Testing antioxidant properties of selected acetylcholinesterase inhibitors
Kucková, Jana ; Vopršalová, Marie (advisor) ; Herink, Josef (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology & Toxicology Student: Jana Kucková Supervisor: PharmDr. Marie Vopršalová, CSc. Title of diploma thesis: Testing antioxidant properties of selected acetylcholinesterase inhibitors Very widespread Alzheimer's disease is typical by a complex pathology. Its causality is not clearly understood. There is increasing discussion due to the negative impact of free radicals on this disease formation. There are testing new substances that have also antioxidant properties, in addition to their classical effects. The aim of this diploma thesis is spectrophotometric testing of antioxidant properties of selected acetylcholinesterase inhibitors. It is based on DPPH test where the presence of antioxidants with antiradical activity causes the reduction of the color stable 2,2-diphenyl-1- picrylhydrazyl (DPPH) radical to a colorless molecule. The principle of the method is the measurement of decrease in absorbance (decolorization) of selected substances that are directly proportional to the antioxidant (antiradical) efficacy of the analyzed inhibitors. It focuses on twelve samples, Phenothiazine, which is the leader structure of new inhibitors synthesis, and two standards. Antioxidant activity is expressed as the effective...
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In vivo evaluation of the efficacy of the novel reactivator against tabun
Kuzmiaková, Natália ; Vopršalová, Marie (advisor) ; Hrdina, Radomír (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Pharmacology and Toxicology Candidate: Natália Kuzmiaková Supervisor: PharmDr. Marie Vopršalová, CSc . Consultant: mjr. PharmDr. Vendula Hepnarová, Ph.D. Title of diploma thesis: In vivo evaluation of the efficacy of the novel reactivator against tabun. This study tackles the problem of irreversible inhibition of acetylcholinesterase (AChE). This enzyme degrades neurotransmitter acetylcholine (ACh), wich ensures transmisson of nerve impulses in central nervous system and in periphery. Organophospates (OP) are substances that cause irreversible blocade of AChE and that susubsequently leads to accumulation of AChE in synapses and inducing of muscarinic and nicotinic effects for life threatening condition. Oximic nature reactivators shown to this day the gratest potencial in inhibiting OP bond with AChE. Because reactivation abilities of to date synthesided oxime are not sufficient, new reactivators are being researched. The doal of my work was to test the potencial to reactivate AChe one of them (precisely oxime K 870). The method i used was colorimetric Ellman method modified by Bajgar, where the activity of AChE after reactivation was measured by absorbance in brain, diaphragm and blood of modeled orgamisms. The...
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Testing antioxidant properties of selected acetylcholinesterase inhibitors
Kucková, Jana ; Vopršalová, Marie (advisor) ; Herink, Josef (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology & Toxicology Student: Jana Kucková Supervisor: PharmDr. Marie Vopršalová, CSc. Title of diploma thesis: Testing antioxidant properties of selected acetylcholinesterase inhibitors Very widespread Alzheimer's disease is typical by a complex pathology. Its causality is not clearly understood. There is increasing discussion due to the negative impact of free radicals on this disease formation. There are testing new substances that have also antioxidant properties, in addition to their classical effects. The aim of this diploma thesis is spectrophotometric testing of antioxidant properties of selected acetylcholinesterase inhibitors. It is based on DPPH test where the presence of antioxidants with antiradical activity causes the reduction of the color stable 2,2-diphenyl-1- picrylhydrazyl (DPPH) radical to a colorless molecule. The principle of the method is the measurement of decrease in absorbance (decolorization) of selected substances that are directly proportional to the antioxidant (antiradical) efficacy of the analyzed inhibitors. It focuses on twelve samples, Phenothiazine, which is the leader structure of new inhibitors synthesis, and two standards. Antioxidant activity is expressed as the effective...
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Testing the efficacy of potential therapeutics for Alzheimer,s disease
Dolejšová, Adéla ; Herink, Josef (advisor) ; Vopršalová, Marie (referee)
Adéla Dolejšová Testing the efficacy of potential therapeutics for Alzheimer,s disease Charles University in Prague, Faculty of Pharmacy in Hradec Kralove Pharmacy The aim of this thesis was to find out whether already implemented Ellman's method, which is used to analyse irreversible inhibitors AChE, is going to be a suitable technique for measuring reversible inhibitors. Furthermore, the efficiency of newly synthesized AChE inhibitors was established. These inhibitors will be used for treating AD or as prophylaxis against neural paralytic substances. Moreover, it was compared affect the efficacy of AChE inhibitors after intramuscular and intraperitoneal administration. The measurements were done in vivo on potkan species Wistar. In the first experiment standard AChE (tacrin, 7-MEOTA, donepezil, rivastigmin) inhibitors were applied to verify the method. In the second experiment the newly synthesizes AChE (K 298, K 344, K 474) inhibitors were medicine. The results confirmed the effectiveness of the tested method on commonly used inhibitors such as donepezil and rivastigmin. Out of the newly synthesized K 298, K 344 and K 474 inhibitors none was proven to have any significant inhibiting activity. Key words: acetylcholinesterase, acetylcholinesterase inhibitors, Alzheimer disease, cholinergic system,...
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