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Transport and biotransformation of selected anthelmintics in lancet fluke
Dokoupilová, Ivana ; Skálová, Lenka (referee) ; Szotáková, Barbora (advisor)
(EN) Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences Candidate: Ivana Dokoupilová Consultant: Doc. Ing. Barbora Szotáková, Ph.D. Title: Transport and biotransformation of selected anthelmintics in lancet fluke Dicrocoeliosis is parasitic infection of small ruminants and mouflon is one of them. Lancet fluke (Dicrocoelium dendriticum) causes this disease. Energetic metabolism is inhibited by therapeutically significant group of pharmaceuticals - benzimidazoles. The aim of this project is to evaluate the transportation of albendazole (ABZ) - representative of benzimidazoles - and its metabolite albendazole sulfoxide (ABZSO) into the bodies of lancet flukes in ex vivo experiment and if lancet fluke biotransform these anthelmintics (ABZ to ABZSO and ABZSO2 (albendazole sulfone)). Lancet fluke (10 parasites) were incubated in medium with anthelmintics for 24 hours. We observed changes of anthelmintics concentration in medium and in parasite's bodies. After the incubation was finished, flukes and medium were separated. Concentration of ABZ and its metabolites was measured on HPLC. Results indicate that albendazole and albendazole sulfoxide are transported to the bodies of flukes. With growing concentration of anthelmintics in medium the concentration...
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The occurrence of Fascioloides magna in deers in South Bohemia
VERNEROVÁ, Kateřina
Giant liver fluke Fascioloides magna is the biggest represenative of flukes in the Czech Republic. This originally North American parasite was brought to Europe with wapiti deers in 1960s. Since that time Fascioloides magna has extended the area of its appearance and its host spectrum a lot. The first appearance of this parasite in the Czech Republic was noted for the first time at a fallow deer which was hunted down in Middle Bohemia in 1930. However in the early 1960s the number of positive findings started to increase at hoofed. In the last decade was observed the expansion of areas of appearance of this fluke in South Bohemia. That is why I decided to make examinations to evaluate the recent appearance of F. magna at deer family in the South Bohemia from March 2009 to January 2010. 74 samples of dropping of a deer from three different areas (Českobudějovicko, Třeboňsko and Šumava national park) were collected and examined and only in the sample from Šumava national park were proved the ovulums of F. magna. Then I examined 11 livers of deers which were hunted down in Šumava national park. In all these livers were found macroscopic changes. In all these examined livers was also finding of fluke F. magna in number from 1 to 72. From the reached results follows that the problems of appearance of F. magna is in the Czech Republic still actual and it is necessery to count with the extending area of appearance of this parasite in the future. Edification among hunting community and the use of information from trained people who make the primary examination of animals after hunting down are possible ways to catch up appearance and expansion of this serious parasite at hoofed.
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Effect of albendazole on activity of biotransformation enzymes in lancet fluke
Hradecká, Aneta ; Skálová, Lenka (referee) ; Szotáková, Barbora (advisor)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences Title, name, surname of aspirant: Aneta Hradecká Title, name, surname of supervizor: Doc. Ing. Barbora Szotáková, Ph.D. Title of diploma thesis: Effect of albendazole on activity of biotransformations enzymes in lancet fluke Disease caused by lancet flukes, dicrocoeliosis, can lead to dicrease of ruminants utility and consequently to economic loses. Albendazole (the benzimidazole anthelmentic) is one of the most important drugs being used in therapy of dicrocoeliosis. Because of the need to use high and repeated dosage of albendazole, a drug resistance can occure. The aim of present thesis was to determine the influence of albendazole on lancet fluke biotransformation enzyme activity. In this experiment, lancet flukes isolated from the liver of mouflons were used. One group of lancet flukes was incubated with albendazole, another group was used as a control sample. The enzyme activity of chosen enzymes (flavine-containing monooxygenases, carbonyl-reducing enzymes, glutathione S-transferases, UDP-glucuronosyl transferases, UDP-glucosyl transferases) was determined in cytosolic fraction, mitochondria and microsomes of both groups of parazites. In the majority of cases, albendazole did not affect the...
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Defence mechanisms of lancet fluke against effects of anthelmintics
Ballóková, Anna ; Vokřál, Ivan (referee) ; Szotáková, Barbora (advisor)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences Candidate: Anna Ballóková Supervisor: Doc. Ing. Barbora Szotáková, Ph.D. Title of diploma thesis: Defence mechanisms of lancet fluke against effects of anthelmintics Dicroceliosis, helminthosis caused by Dicrocoelium dendriticum (lancet fluke), is worldwide spread infection of small ruminants. The only way of effective control of this parasitosis is in administration of anthelmintics. In lancet fluke, benzimidazole anthelmintic albendazole metabolism via enzymatic sulfoxidation was found but no information about albendazole oxidases is available. The aim of this work was to identify enzymes involved in the metabolism of albendazole in Dicrocoelium dendriticum isolated from naturally infected mouflons (Ovis musimon). To determinate the involved enzymes some of the specific inhibitors were used. The only effective inhibitors used in this work were α-nafthylthiourea and methimazole, specific inhibitors of flavin-containing monooxygenases. Indole-3-carbinole, used as the specific inhibitor of the same enzymatic system, was without any effect. Other inhibitors were used: 3-amino-1,2,4-triazole for catalase, diethyldithiocarbamate and octylamine for cytochrome P450 and salicylohydroxamic acid and...
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The use of LC/MS for the Study of Biotransformation of Xenobiotics in Helminths
Vokřál, Ivan ; Szotáková, Barbora (advisor) ; Lísa, Miroslav (referee) ; Horák, Petr (referee)
Charles University in Prague, Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences Candidate Mgr. Ivan Vokřál Supervisor Doc. Ing. Barbora Szotáková, Ph.D. Title of Doctoral Thesis The use of LC/MS for the study of biotransformation of xenobiotics in helminths Annually, parasites cause many losses regarding not only human lives but also the livestock. One of the most effective weapons that can be used against them are anthelmintics. However, in many cases anthelmintics cease to work and resistance development occurs. One of the possible mechanisms of resistance is the biotransformation of the drug to ineffective or less active products by the parasite. The aim of this work was to bring new knowledge about the biotransformation of drugs in helminths. Emphasis was given to the relationship between biotransformation and the resistance of parasites against anthelmintic drugs. A possible technique to achieve this goal is to study directly the products of biotransformation, i.e. metabolites. As this issue is nowadays most frequently solved by liquid chromatography and mass spectrometry, we used this technique to meet our goals. Biotransformation was studied in representatives of tapeworms, flukes and roundworms. Where possible, economically important representatives as Barber's pole...
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The effect of dicrocoeliosis on biotransformation of anthelmintics in mouflon
Srpová, Veronika ; Szotáková, Barbora (advisor) ; Lamka, Jiří (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences Field: Patobiochemistry and Xenobiochemistry Candidate: Mgr. Veronika Srpová Consultant: Ing. Barbora Szotáková, Ph.D. Title: The effect of dicrocoeliosis on biotransformation of anthelmintics in mouflon Parasitic infections can modify the host's ability to metabolize drugs and other xenobiotics by altering the biotransformation enzymes. These changes may have various pharmacological, toxicological or physiological consequences. In our study, in vitro metabolism of albendazole, albendazole sulfoxide and flubendazole was tested and compared in non-infected mouflons and in mouflons infected by lancet fluke (Dicrocoelium dendriticum). Two groups of 5-7 years old mouflon ewes (Ovis musimon) were used for our study. Animals in the first group were parasitologically negative and the second group consisted of fluke positive animals. Subcellular fractions of liver homogenates from non-infected and Dicrocoelium-infected mouflons were isolated. The hepatic microsomal and cytosolic fractions were incubated with albendazole, albendazole sulfoxide or flubendazole. The anthelmintics and their metabolites were analyzed using HPLC. Apparent kinetic parameters (Vmax and Km) of biotransformation reactions were...
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