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Effect of monepantel on the expression of selected enzymes in Haemonchus contortus
Jelenková, Klára ; Matoušková, Petra (advisor) ; Raisová Stuchlíková, Lucie (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences Candidate: Klára Jelenková Supervisor: Ing. Petra Matoušková, Ph.D. Title of diploma thesis: Effect of monepantel on the expression of selected enzymes in Haemonchus Contortus Barber's pole worm (Haemonchus contortus) is parasitic nematode which is the cause of haemonchosis, worldwide distributed disease of small ruminants leading to decrease in productivity and in many cases even to animals death. For prevention and treatment of this disease are used drugs for a long time - anthelmintics. Due to their frequent use and lack of innovation in this group of drugs parasites have gradually built an extensive resistance to these drugs. New hope in therapy of haemonchoses is monepantel, drug belonging to aminoacetonitrile derivatives which have unique mechanism of action. This drug was launched more than 25 years after registration of the last drug from the group of anthelmintics. Despite the initial great success information about occurrence of resistance often appear in recent years. Current knowledge about the mechanisms of resistance development and the factors that influence them is as well as information about drug action at the molecular level still insufficient. To limit the development of...
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Biotransformation enzymes and metabolism of anthelmintics in Fascioloides magna
Rejšková, Lenka ; Szotáková, Barbora (advisor) ; Raisová Stuchlíková, Lucie (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences Candidate: Mgr. Lenka Rejšková Supervisor: doc. Ing. Barbora Szotáková, Ph.D. Consultant: Mgr. Lukáš Prchal Title of rigorous thesis: Biotransformation enzymes and metabolism of drugs in Fascioloides magna Biotransformation of xenobiotics including drugs is detoxifying ability of all organisms and it leads to positive and/or negative effects of pharmacotherapy. Each animal species is distinguished by quantitative and qualitative differences in biotransformation enzymes. Knowledge of these differences is crucial for effective and safe pharmacotherapy. It has become vital particularly when drug resistance is becoming a worldwide problem. This study was focused on parasite species Fascioloides magna which is responsible for extensive deaths of ruminants. In spite of this fact, there is lack of detailed information on its metabolism of anthelmintics or metabolism in general. The aim of this study was to find out biotransformation of anthelmintics in F. magna and activity of biotransformation enzymes in subcellular fractions from F. magna in the presence of model substrates. On the basis of fact that there were obtained activities of oxidative enzymes (FMO, GPx, CAT, Px, TrxR and NQO-1) and conjugation...
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METABOLISM AND EFFECTS OF NEW ANTHELMINTIC DRUG IN HELMINTHS AND ITS HOSTS
Stuchlíková, Lucie ; Skálová, Lenka (advisor) ; Kučera, Radim (referee) ; Machala, Miroslav (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences Candidate Mgr. Lucie STUCHLÍKOVÁ Supervisor prof. RNDr. Lenka SKÁLOVÁ, Ph.D. Title of Doctoral Thesis METABOLISM AND EFFECTS OF NEW ANTHELMINTIC DRUG IN HELMINTHS AND ITS HOSTS Diseases caused by helminths, called helminthoses, are one of the most serious problems in veterinary and human medicine. These diseases are treated by anthelmintics but their effectiveness is often not sufficient due to resistance of helminths against common anthelmintics. The global anthelmintic resistance encouraged the developing of new drugs with a different mode of action. Monepantel (MOP) belongs to a new class of anthelmintic drugs known as amino- acetonitrile derivatives (AADs) that act on the nicotinic acetylcholine receptors. In 2011, MOP was approved for the treatment of gastrointestinal diseases caused by nematodes in the veterinary practice in the Czech Republic. It is produced commercially under the trade name Zolvix® (Novartis AG). The aim of this doctoral thesis was to study metabolism and effects of MOP and other AADs in order to contribute to the global research in this field. For this purpose, adults nematodes Haemonchus contortus (the sensitive strain ISE and the resistant strain WR) and its hosts Ovis...
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METABOLISM AND EFFECTS OF NEW ANTHELMINTIC DRUG IN HELMINTHS AND ITS HOSTS
Stuchlíková, Lucie ; Skálová, Lenka (advisor) ; Kučera, Radim (referee) ; Machala, Miroslav (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences Candidate Mgr. Lucie STUCHLÍKOVÁ Supervisor prof. RNDr. Lenka SKÁLOVÁ, Ph.D. Title of Doctoral Thesis METABOLISM AND EFFECTS OF NEW ANTHELMINTIC DRUG IN HELMINTHS AND ITS HOSTS Diseases caused by helminths, called helminthoses, are one of the most serious problems in veterinary and human medicine. These diseases are treated by anthelmintics but their effectiveness is often not sufficient due to resistance of helminths against common anthelmintics. The global anthelmintic resistance encouraged the developing of new drugs with a different mode of action. Monepantel (MOP) belongs to a new class of anthelmintic drugs known as amino- acetonitrile derivatives (AADs) that act on the nicotinic acetylcholine receptors. In 2011, MOP was approved for the treatment of gastrointestinal diseases caused by nematodes in the veterinary practice in the Czech Republic. It is produced commercially under the trade name Zolvix® (Novartis AG). The aim of this doctoral thesis was to study metabolism and effects of MOP and other AADs in order to contribute to the global research in this field. For this purpose, adults nematodes Haemonchus contortus (the sensitive strain ISE and the resistant strain WR) and its hosts Ovis...
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Synthesis of isotopically labeled ketamine
Stuchlíková, Lucie ; Lešetický, Ladislav (advisor) ; Smrček, Stanislav (referee)
In this work were synthesized ketamine isotopomers. Ketamine is used in human medicine and veterinary sectors. It has very broad spectrum of pharmacological effects: anesthetic, analgesic, hallucinogenic, bronchodilator, cardiovascular and antidepressive, which is currently in the research. At first was synthesized precursor of ketamine, N- desmethylketamine which was subsequently labeled the deuterium, tritium and carbon- 14. For the determination of purity and identity mass spectrometry and nuclear magnetic resonance spectroscopy were used. KEY WORDS synthesis of ketamine, ketamine, N-desmethylketamine, nor-ketamine, isotopically labeled ketamine, deuterium, tritium, carbon-14.
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Systémový přístup ke snižování zatížení životního prostředí v souvislosti s výstavbou a provozem budov‚ s důrazem na stavebně-energetické souvislosti
EkoWATT, Praha ; Knápek, Jaroslav ; Kabele, Karel ; Stuchlíková, Lucie ; Šašková, Dana ; Urbánková, Veronika ; Kalčev, Petr ; Staněk, Kamil ; Šafařík, Miroslav ; Truxa, Jan ; Srdečný, Karel ; Beranovský, Jiří ; Tywoniak, Jan ; Lupíšek, Antonín ; Hudcová, Lenka ; Macholda, František
Dokumentace k rodinným domům z hlediska enegetické náročnosti.
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Systémový přístup ke snižování zatížení životního prostředí v souvislosti s výstavbou a provozem budov‚ s důrazem na stavebně-energetické souvislosti
EkoWATT, Praha ; Knápek, Jaroslav ; Kabele, Karel ; Stuchlíková, Lucie ; Šašková, Dana ; Urbánková, Veronika ; Kalčev, Petr ; Staněk, Kamil ; Šafařík, Miroslav ; Truxa, Jan ; Srdečný, Karel ; Beranovský, Jiří ; Tywoniak, Jan ; Lupíšek, Antonín ; Hudcová, Lenka ; Macholda, František
Studie se zabývá energetickou a environmentální náročností staveb a možnostmi, jak ji ekonomicky efektivně snížit. Byly shromážděny a analyzovány údaje ze tří zdrojů: z průzkumu na stavebních úřadech, ze vzorku energetických auditů a z většího množství projektů reálných budov. byly vytvořeny modely budov, které hodnotí budovy jako celek. Do modelu byly zahrnuty potřeby energií na vytápění, ohřev vody a provoz elektrospotřebičů, odpovídající provozní náklady, potřebné reinvestice v průběhu sledované životnosti objektu a environmentální důsledky jeho provozu. Závěrečná zpráva podává celkový pohled na možnosti ovlivnění obvyklého způsobu navrhování staveb z hlediska všech účastníků tohoto procesu, a to v rámci technických, ekonomických a organizačních možností účastníků.
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