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Biotransformation of selected anthelmintics in Haemonchus contortus
Sečkařová, Anna ; Raisová Stuchlíková, Lucie (advisor) ; Skarka, Adam (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences Candidate: Anna Sečkařová Supervisor: RNDr. Lucie Raisová Stuchlíková, Ph.D. Title of diploma thesis: Biotransformation of selected anthelmintics in Haemonchus contortus Resistance to benzimidazole anthelmintics is one of the main problems of small ruminant producers. The most problematic parasite of goats and sheep is the bloodsucking barber's pole worm, Haemonchus contortus. This parasite is responsible for considerable losses every year. The goal of this thesis was an analysis of the metabolism of a few selected benzimidazoles (albendazole, ABZ; ricobendazole, RCB and flubendazole, FLU) in H. contortus. The metabolism of male and female worms and a susceptible ISE strain (Inbred Susceptible Edinburgh, MHco3) with a resistant IRE strain (Inbred Resistant Edinburgh, MHco5) were compared. For metabolite detection, ultra-high-performance liquid chromatography with mass spectrometry (UHPLC/MS) was used. 12 metabolites of FLU, 9 metabolites of ABZ and 7 metabolites of RCB were identified. From the identified metabolites, schemes of metabolism were proposed. In metabolism comparisons, significant differences between sexes and strains were found. Female worms metabolized tested anthelmintics more...
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The effect of selected sesquiterpenes on antioxidant enzymes in Caco-2 cell line
Janíček, Tomáš ; Svobodová, Hana (advisor) ; Raisová Stuchlíková, Lucie (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences Candidate: Tomáš Janíček Supervisor: PharmDr. Hana Svobodová, Ph.D. Title of diploma thesis: The effect of selected sesquiterpenes on antioxidant enzymes in Caco-2 cell line Colorectal carcinoma is a very frequent type of malignant neoplasms, while the Czech Republic has the sixth highest incidence of this disease globally. Current chemotherapy is often not an ideal option, and there is an effort to find substances that could replace it or reduce its dosage, and therefore its adverse effects. A promising source of natural substances is the Chinese tree Myrica rubra, whose extracts have inhibited the proliferation of many tumour cell lines. Also, in several colon carcinoma cell lines, the growth inhibition was observed after their cultivation with the essential oil from the M. rubra's leaves (SMR), with the Caco-2 line being the most sensitive. The main sesquiterpenes of SMR β-caryophyllene, α-humulene (α-HUM), trans-nerolidol (t-NER) and valencene proved the antiproliferative effects on this cell line too. α-HUM and t-NER showed the formation of reactive oxygen species (ROS) on colon carcinoma cells. The aim of our work was to find out how SMR, α-HUM and t-NER at concentrations of 25 and 50 μg/ml, influence...
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Co2+ loaded block copolymer micelles: Preparation and their uptake into macrophages
Měrková, Veronika ; Jansová, Hana (advisor) ; Raisová Stuchlíková, Lucie (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences Friedrich Schiller University Jena Faculty of Chemistry and Earth Sciences Institute for Organic and Macromolecular Chemistry Candidate: Veronika Měrková Supervisors: PharmDr. Hana Jansová, Ph.D., Prof. Dr. Felix H. Schacher Title of diploma thesis: Co2+ loaded block copolymer micelles: Preparation and their uptake into macrophages Since lots of patients suffer from post-operative infections resulting in sepsis, there were attempts to modulate immune system response in order to treat this pathological state. Cobalt is a biogenic trace element, however its direct administration may cause immunological reactions. The immune response can be inflammatory or anti- inflammatory mediated by macrophages (MΦ). Both are responsible for specific actions, regarding MΦ activation and cytokine release. The aim of this study was to provoke such response in MΦ and therefore to possibly control the inflammatory process. Nevertheless, free cobalt ions are toxic. In order to find a suitable and safe way of cobalt administration, the triblock terpolymer PEO-b-PAGECOOH-b-PtBGE was synthesized and assembled into micelles in aqueous solution. Eventually the micelles were loaded with cobalt chloride to facilitate the detection in a...
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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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In vitro cultivation of tapeworm Hymenolepis diminuta - 2
Jandura, Dominik ; Vokřál, Ivan (advisor) ; Raisová Stuchlíková, Lucie (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Pharmacology & Toxicology Student: Dominik Jandura Supervisor: PharmDr. Ivan Vokřál, Ph.D. Title of diploma thesis: In vitro cultivation of tapeworm Hymenolepis diminuta - 2 Aim of this diploma thesis was to obtain cycticercoids of the rat tapeworm (Hymenolepis diminuta), excyst them and find out the conditions for the maximal in vitro incubation period. As the intermediate host mealworm beetle (Tenebrio molitor) infected by the rat feces containing tapeworm eggs was used. Excystment was done using L-cystein and sodium tauroglycocholate. Excysted larvae were cultured in vitro (37 řC, 5 % CO2) in RPMI 1640 medium enriched with other substances chosen according previously published methods. Mainly sheep, mouse or rat liver extracts eventually in combination with yeast extract and sheep bile were used. The effect of tested substances on the cultivation was evaluated by measuring of the tapeworm's growth. The best effect on the grow of the tapeworms was observed using medium containing serum, yeast extract and sheep liver extract where tapeworms achieved length of 1561 µm after 16 days of incubation. The further growth was limited by appearance of pathologic formations.
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The pharmacokinetics of ivermectin in the feces of Ovis ammon
Lokvencová, Kateřina ; Raisová Stuchlíková, Lucie (advisor) ; Matoušková, Petra (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences Candidate: Mgr. Kateřina Lokvencová Tutor: RNDr. Lucie Raisová Stuchlíková, Ph.D. Title of Thesis: The pharmacokinetics of ivermectin in the feces of Ovis ammon Keywords: Anthelmintics, ivermectin, sheep, pharmacokinetics, excretion Infection with internal parasites is one of the most common diseases in sheep worldwide and causes significant economic losses. The nematode (Haemonchus contortus) is among to the particularly problematic representatives. Anthelmintics are used to treat helmintoses and they are divided into the several classes. The class of macrocyclic lactones includes ivermectin (IVE), which is especially popular for wide range of efficacy and low toxicity. However, the study of IVE pharmacokinetics is difficult, because it depends on many factors. Considerable attention is directed to the elimination of IVE, because its residuals in dung can adversely affect the environment and thus promote the emergence of resistance. The aim of this study was study of the elimination of IVE in sheep, especially the study of excretion profile. IVE (dose 0.2 mg/kg of body weight) was subcutaneously administered to sheep, followed by sampling of faeces at specified intervals. Ultra-high performance...
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The impact of selected sesquiterpenes on antioxidant enzymes in HT-29 cell line
Junková, Martina ; Raisová Stuchlíková, Lucie (advisor) ; Jansová, Hana (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences Candidate: Martina Junková Tutor: RNDr. Lucie Raisová Stuchlíková, Ph.D. Title: Effect of selected sesquiterpenes on antioxidant enzymes in the HT-29 cell line Colorectal cancer is one of the most common cancer type in Czech republic. The oncological treatment causes frequent side effects, what result in hard accepting by patients. There is also emerging resistance to classical chemotherapy (5-fluorouracil). During searching new alternatives, some promising natural substances became a subject of researches. The subtropical tree Myrica rubra and its extracts contain many biologically active substances, which are studied among others for their anti-cancer and antiproliferative effects. β-caryophyllene (BCP), β-caryophyllenoxid (CAO), α- humulene (HUM), trans-nerolidol (NER) and valencen (Val) belong to main sesquiterpenes in this essential oil Myrica rubra. In our study, effect of essential oil Myrica rubra, HUM and NER, in concentrations of 25 and 50 μg/ml, were examined after a 24-hours incubation of the HT-29 cell line on the activity of antioxidant enzymes, their transcription and amount of proteins. Monitored enzymes were glutathione peroxidase (GPx), glutathione reductase (GR),...
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Co2+ loaded block copolymer micelles: Preparation and their uptake into macrophages
Měrková, Veronika ; Jansová, Hana (advisor) ; Raisová Stuchlíková, Lucie (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences Friedrich Schiller University Jena Faculty of Chemistry and Earth Sciences Institute for Organic and Macromolecular Chemistry Candidate: Veronika Měrková Supervisors: PharmDr. Hana Jansová, Ph.D., Prof. Dr. Felix H. Schacher Title of diploma thesis: Co2+ loaded block copolymer micelles: Preparation and their uptake into macrophages Since lots of patients suffer from post-operative infections resulting in sepsis, there were attempts to modulate immune system response in order to treat this pathological state. Cobalt is a biogenic trace element, however its direct administration may cause immunological reactions. The immune response can be inflammatory or anti- inflammatory mediated by macrophages (MΦ). Both are responsible for specific actions, regarding MΦ activation and cytokine release. The aim of this study was to provoke such response in MΦ and therefore to possibly control the inflammatory process. Nevertheless, free cobalt ions are toxic. In order to find a suitable and safe way of cobalt administration, the triblock terpolymer PEO-b-PAGECOOH-b-PtBGE was synthesized and assembled into micelles in aqueous solution. Eventually the micelles were loaded with cobalt chloride to facilitate the detection in a...
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The effect of selected sesquiterpenes on antioxidant enzymes in Caco-2 cell line
Janíček, Tomáš ; Svobodová, Hana (advisor) ; Raisová Stuchlíková, Lucie (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences Candidate: Tomáš Janíček Supervisor: PharmDr. Hana Svobodová, Ph.D. Title of diploma thesis: The effect of selected sesquiterpenes on antioxidant enzymes in Caco-2 cell line Colorectal carcinoma is a very frequent type of malignant neoplasms, while the Czech Republic has the sixth highest incidence of this disease globally. Current chemotherapy is often not an ideal option, and there is an effort to find substances that could replace it or reduce its dosage, and therefore its adverse effects. A promising source of natural substances is the Chinese tree Myrica rubra, whose extracts have inhibited the proliferation of many tumour cell lines. Also, in several colon carcinoma cell lines, the growth inhibition was observed after their cultivation with the essential oil from the M. rubra's leaves (SMR), with the Caco-2 line being the most sensitive. The main sesquiterpenes of SMR β-caryophyllene, α-humulene (α-HUM), trans-nerolidol (t-NER) and valencene proved the antiproliferative effects on this cell line too. α-HUM and t-NER showed the formation of reactive oxygen species (ROS) on colon carcinoma cells. The aim of our work was to find out how SMR, α-HUM and t-NER at concentrations of 25 and 50 μg/ml, influence...
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