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Methodology for identification and classification of areas with landscape values: Methodology certified by the Ministry of Culture
Kuča, Karel ; Kupka, Jiří ; Vorel, Ivan ; Vondráčková, Simona
The methodology, which is closely related to the previous results of interdisciplinary cooperation of the team of authors in the field of historical cultural landscape, in particular to the methodology of the Typology of Historical Cultural Landscape of the Czech Republic, is intended to serve, among others, for the definition of the newly introduced in 2018 spatial analytical documents of municipalities No. 11: Urban and Landscape Values. An important part of the methodology is the description of the method that ensures unambiguous and correct classification of any territory into one of the value categories (including territories that do not show landscape values). The procedure is described in three basic steps (stages), including the procedure for the designation itself. The novelty and uniqueness of the methodology lies in the creation of a professional basis for the delineation of areas with landscape values, which has been lacking in spatial planning practice so far. The methodology is based on more than 30 years of experience of the authors in field surveys and evaluation of historic cultural landscapes (and urbanism) in the Czech Republic and monitoring of relevant literature and expert discussions at national and international level.
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Cholinesterase activity following experimentally induced organophosphorus poisoning.
Svobodová, Irena ; Herink, Josef (advisor) ; Kuča, Kamil (referee)
The aim of present work was a comparison of effectiveness of oximes chosen in the experimental therapy of nerve agents intoxication (soman and russian VX). All experiments were performed in male Wistar rats. All oximes tested were administered intramuscularly either in a separate injection or in combination with atropine. The preparation of the brain parts for determination of acetylcholinesterase was performed in several time intervals after drugs tested administration. Antidotal potency of oxime HI-6 was superior in comparison with the rest of oximes tested.
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Synthesis of bisquaternary asymmetrical reactivators of acetylcholinesterase
Komlóová, Markéta ; Doležal, Martin (advisor) ; Kuča, Kamil (referee)
Markéta Komlóová: Synthesis of bisquarternary asymmetrical reactivators of acetylcholinesterase Nine potential bisquaternary reactivators of AChE have been prepared and their reactivation activity against paraoxon or tabun-inhibited enzyme has been tested in vitro. Three reactivators of AChE proved to be suitable for further testing against paraoxon. One of these compounds also demonstrated satisfactory efficiency when reacting against tabun. The reactivation abilities of prepared compounds depend on structural factors such as the presence of oxime group, its location, the presence of quaternary nitrogen and other functional groups. Also four monoquaternary inhibitors have been prepared and their inhibitive activity tested in vitro.
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Issues of the Cholinesterase Inhibition by the Selected Organophosphorous Pesticides In Vitro
Lázenská, Helena ; Opletalová, Veronika (advisor) ; Kuča, Kamil (referee)
QUESTIONS OF THE IN VITRO INHIBITION OF CHOLINESTERASES BY SELECTED ORGANOPHOSPHORUS PESTICIDES Helena Lázenská Department of Pharmaceutical Chemistry and Drug Control, Faculty of Pharmacy in Hradec Kralove, Charles University in Prague, Heyrovskeho 1203, 500 05, Hradec Kralove, Czech Republic. The aim of this study was to describe organophosphorus inhibitors paraoxone, DDVP and DFP from the aspect of the kinetics of their reaction with human erythrocyte acetylcholinesterase (AChE) and plasma butyrylcholinesterase (BuChE), to find IC50, and to test the in vitro potency of five selected oximes (pralidoxime, methoxime, trimedoxime, obidoxime and HI-6) to reactivate AChE and BuChE inhibited by three mentioned organophosphorus inhibitors. The inhibition of AChE and BuChE was performed by incubation with organophosphorus inhibitors at a convenient concentration and such time, that would result in about 90% activity of an enzyme. A solution of a reactivator at a final concentration 1 μM or 10 μM was added to an enzyme, after 10 min of reactivation, a solution of a substrate - acetylthiocholine-iodide or butyrylthiocholine-iodide was added, and the activity of an enzyme was measured by the spectrophotometric Ellman's method. The experiment was performed at 25 žC, pH 7,4 and in a 0,1 M phosphate buffer. According...
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Biological activity of plant metabolites III. Influence of alkaloids from Chelidonium majus L. on acetylcholinesterase
Kubincová, Dagmar ; Opletal, Lubomír (advisor) ; Kuča, Kamil (referee)
SOUHRN Spolu s ostatními diplomantkami (Šárkou Brožovou, Janou Nagyovou a Evou Vítkovou) jsem provedla extrakci 41,8 kg suché nati s kořeny. Primární extrakt jsme vyčistily filtrací a následným oddestilováním rozpouštědla na vakuové odparce. Dále jsme připravily sekvenčním postupem výtřepky s jednotlivými typy alkaloidů: šlo o dva diethyletherové výtřepky (získané po předchozí alkalizaci primárního extraktu uhličitanem sodným a hydroxidem draselným), které byly následně okyseleny kyselinou chlorovodíkovou, vzniklé kvartérní jodidy po přidání jodidu draselného vytřepány chloroformem a po následné alkalizaci extraktu amoniakem získány další kvartérní jodidy vytřepáním do směsi chloroform + ethanol 8,5:1,5. Já jsem se zabývala výtřepkem B, který obsahoval silně basické alkaloidy. Provedla jsem separaci výtřepku B pomocí sloupcové chromatografie. Zpracovávala jsem frakci 27- 46, jejíž odparek jsem po vysušení rozdělila na dvě části. První část (0,02 g) byla podrobena barevným reakcím s činidly, které prokázaly, že izolovaný alkaloid CH-M/B-1 je berberin.Dále jsem změřila teplotu tání Z druhé části odparku jsem získala 0,346 g žlutého prášku, který byl v závěru práce podroben testu vlivu látky na aktivitu AChE. Z naměřené hodnoty IC50= 0,221 (0,146- 0,228) μM je patrné, že látka CH-M/B-1 je vysoce aktivní v...
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Synthesis of precursors for biologically active lactones IV.
Bémová, Hana ; Opletalová, Veronika (advisor) ; Kuča, Kamil (referee)
Charles University in Prague, Faculty of Pharmacy in Hradec Kralove Department of Pharmaceutical Chemistry and Drug Control SYNTHESIS OF PRECURSORS FOR BIOLOGICALLY ACTIVE LACTONES IV. Rigorous Thesis Hana Piskacova A high width of biological activity of natural or synthetic unsaturated five membered lactones from the family of furan-2(5H)-ones, is the main reason why to synthesize new substances of this structure. The introductory part of the thesis deals with antineoplastic natural compounds of this type. Except of antitumour activity some unsaturated five membered lactones exhibit antifungal, antiviral, antibacterial effects, or inhibit the synthesis of cholesterol, for example. The experimental project is an extension of my diploma thesis concerned with the synthesis of precursors for lactones. These precursors - methyl (E)- and (Z)-2-bromo-5- (subst.)arylpent-2-en-4-ynoates - were prepared by Sonogashira couplings. The parent substances for couplings were arylethynes (1-ethynyl-4-(methoxymethoxy)benzen, 1-ethynyl-2-nitrobenzene, 3-ethynylaniline, 2-ethynylpyridine) and methylesters of dihalogenated prop-2-enoic acid. The dominant products of the couplings were β-monoalkynylated esters, apart from them side products of homocouplings were obtained. Reactions of E-methylesters of dihalogenated...
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Electrosynthesis of Delta-Valero Lactones
Pochopová, Lenka ; Kubíček, Vladimír (advisor) ; Kuča, Kamil (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of pharmaceutical chemistry Candidate: Mgr. Pochopová Lenka Consultant: Ing. Kubíček Vladimír, CSc. Tittle of Thesis: ,,ELECTROSYNTHESIS OF DELTA-VALERO LACTONES" In this project electrolysis has been used as a method for a synthesis of new compounds. The main aim is cathodic reduction of the carbon-chlorine bond in a series of aldol trichloroacetates. Formed carbanion would form a 6 member ring by attaching the carbonyl group. Two structures can be formed: α, α-dichloro-β-hydroxy-δ-lactones and α, β-unsaturated-α-chloro -δ-lactones from the starting esters using electrolysis. The whole process was performed at controlled potential in a separated cell, on mercury pool as a cathode and platinum as an anode in an argon atmosphere with dichloromethane/tetraethylamonium system. During the process two electrons have been passed. The synthesized lactones are completely new compounds. In this report also electrochemical and spectroscopy properties of those compounds have been characterized to provide for their other use.
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Methodology for the Classification and Evaluation of Industrial Heritage: Water Management
Caletka, Martin ; Dráb, Aleš ; Dzuráková, Miriam ; Forejtníková, Milena ; Hronek, David ; Hudcová, Hana ; Julínek, Tomáš ; Račoch, Radka ; Rozkošný, Miloš ; Kuča, Karel ; Borovcová, Alena ; Drnek, Kryštof ; Kolka, Miroslav ; Matěj, Miloš ; Ryšková, Michaela ; Urbánek, Radim ; Frajer, Jindřich ; Létal, Aleš ; Pavelková, Renata ; Kotari, Sixtus Bolom ; Sviták Zbyněk ; Vyskočil, Aleš
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