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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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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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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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Analysis of arginine and its methylated derivatives in clinical samples using LC-MS/MS
Prokop, Pavel ; Boušová, Iva (advisor) ; Raisová Stuchlíková, Lucie (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences Candidate: Bc. Pavel Prokop, DiS. Supervisor: doc. PharmDr. Iva Boušová, Ph.D. Title of diploma thesis: Analysis of arginine and its methylated derivatives in clinical samples using LC-MS/MS Asymmetric dimethylarginine (ADMA) and its enantiomer, symmetric dimethylarginine (SDMA), are naturally occurring amino acids that are generated intracellularly from L-arginine. ADMA is an endogenous competitive inhibitor of nitric oxide synthase. Increased levels of ADMA and SDMA are associated with endothelial dysfunction, hypertension, cardiovascular and renal diseases. Both compounds are accumulating in chronic kidney disease (CKD) patients. The aim of this diploma thesis was to develop and validate a liquid chromatography with tandem mass spectrometry (LC-MS/MS) method for the determination of L-arginine, ADMA and SDMA in human plasma. Subsequently, LC-MS/MS method was compared with enzyme-linked immunosorbent assay (ELISA) and high-performance liquid chromatography with fluorescence detection (HPLC-FL) method. Chromatographic separation was performed on Dionex UltiMate 3000 UHPLC liquid chromatograph, followed by tandem mass spectrometric detection on amaZon SL mass spectrometer. L-Arginine-13 C6, ADMA-d6 and...
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Analysis of arginine and its methylated derivatives in clinical samples using LC-MS/MS
Prokop, Pavel ; Boušová, Iva (advisor) ; Raisová Stuchlíková, Lucie (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences Candidate: Bc. Pavel Prokop, DiS. Supervisor: doc. PharmDr. Iva Boušová, Ph.D. Title of diploma thesis: Analysis of arginine and its methylated derivatives in clinical samples using LC-MS/MS Asymmetric dimethylarginine (ADMA) and its enantiomer, symmetric dimethylarginine (SDMA), are naturally occurring amino acids that are generated intracellularly from L-arginine. ADMA is an endogenous competitive inhibitor of nitric oxide synthase. Increased levels of ADMA and SDMA are associated with endothelial dysfunction, hypertension, cardiovascular and renal diseases. Both compounds are accumulating in chronic kidney disease (CKD) patients. The aim of this diploma thesis was to develop and validate a liquid chromatography with tandem mass spectrometry (LC-MS/MS) method for the determination of L-arginine, ADMA and SDMA in human plasma. Subsequently, LC-MS/MS method was compared with enzyme-linked immunosorbent assay (ELISA) and high-performance liquid chromatography with fluorescence detection (HPLC-FL) method. Chromatographic separation was performed on Dionex UltiMate 3000 UHPLC liquid chromatograph, followed by tandem mass spectrometric detection on amaZon SL mass spectrometer. L-Arginine-13 C6, ADMA-d6 and...
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Metabolism of ivermectine in selected plants
Štumbauerová, Kateřina ; Raisová Stuchlíková, Lucie (advisor) ; Matoušková, Petra (referee)
1 Abstract Charles University in Prague Fakulty of Pharmacy in Hradec Králové Department of Biochemical Sciences Author: Kateřina Štumbauerová Leader: RNDr. Lucie Raisová Stuchlíková Title of diploma thesis: Metabolism of ivermectin in selected plants Ivermectin can enter the environment through the excrement of treated animals like other anthelmintics and it can cause a large number of side effects in the ecosystem, accumulate in plants and affect invertebrates. Due to these causes, resistance of individual parasites can occur. In this work we focused on the study of the biotransformation of ivermectin in common meadow flowers which include thale cress (Arabidopsis thaliana), ribwort plantain (Plantago lanceolata) and soybean (Glycine max). Plants were able to metabolize ivermectin by first phase biotransformation enzymes, producing metabolites that were identified by high performance liquid chromatography-mass spectrometry (UHPLC-MS). Cross-species differences were noticeable, especially in terms of the number of metabolites found in individual plants. The unmetabolized parent compound ivermectin was also detected in plants.
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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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Glycated hemoglobin: one of the indicators of compensation Diabetes mellitus
Vondráčková, Helena ; Raisová Stuchlíková, Lucie (advisor) ; Boušová, Iva (referee)
Diabetes mellitus belongs to the chronic civilization diseases with increasing inter-incidence. This Disease is connected with numerous complications that increase patients mortality and morbidity. The aim of the cure is to compensate and delay the development of especially late complications of diabetes. The bachelor thesis is focused on glycated hemoglobin, which is currently considered the primary method in evaluation of the diabetes mellitus compensation. The theoretical part is focused on basic characteristics and associated complications with the attention paid to the evaluation of the disease compensation. The practical part is focused on methods of determination of glycated hemoglobin, relations among the patients' levels of glycated hemoglobin, average blood glucose and BMI. Key words: Diabetes mellitus, glycated hemoglobin, diabetic retinopathy, diabetic nephropathy, diabetic neuropathy.
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Biotranformation of fenbendazole in soya (Glycine max)
Martínková, Lenka ; Raisová Stuchlíková, Lucie (advisor) ; Matoušková, Petra (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences Candidate: Bc. Lenka Martínková Supervisor: RNDr. Lucie Raisová Stuchlíková, Ph.D. Title of diploma thesis: Biotransformation of fenbedazole in soya (Glycine max) Veterinary drugs are used in large amounts in modern husbandry for treatment and prevention of diseases in animals. Anthelmintics administered to animals enter into environment primarily through its excretion in faeces or urine. Following excretion, drugs may persist in the environment and impact non-target organisms. Plants are able to uptake xenobiotics, including drugs, and detoxify them via biotransformation. However, only drug biotransformation into non-toxic and stable metabolites and their consequent accumulation in plants represent drug detoxification. For that reasons, knowledge of biotransformation pathways of drug in plants is very important. Soybean plants, eventually seeds, are further used in agriculture as feed for cattle and absorbed anthelmintics including their metabolites can enter the food chain. The results showed that fenbendazole entered plant and enzymatic systems of plant were able to biotransform fenbendazole via several reactions. We found differences in the metabolites between the roots, leaves, seeds and pods of soybean.
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