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Assessment of chelating properties of 6,7-dihydroxycoumarin
Kolouch, Jan ; Filipský, Tomáš (advisor) ; Rathouská, Jana (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Pharmacology and Toxicology Candidate: Mgr. Jan Kolouch Consultant: PharmDr. Tomáš Filipský, Ph.D. Title of thesis: Assessment of chelating properties of 6,7-dihydroxycoumarin Iron is an indispensable element in the human body. This element plays irreplaceable role in many metabolic processes, such as transport of oxygen and synthesis of DNA. The essential feature of iron is its ability to transport electrons and facilitation of catalytic reactions. These reactions are realized by redox properties of iron, which naturally occurs at two different oxidation states, i.e. Fe2+ and Fe3+ . Nevertheless, this element can catalyze not only beneficial, but also toxic reactions. One of those is Fenton reaction, which results in the formation of reactive oxygen species that are toxic to the surrounding tissue. In this thesis we have focused on the assessment of chelating properties of 6,7- dihydroxycoumarin (67DHC) at various pH conditions (4.5, 5.5, 6.8 and 7.5) using both competitive and direct UV-Vis spectrophotometry. Further, we have evaluated its reducing activity at pH 4.5 and 5.5. By the analysis of UV-Vis absorption spectra we have found out, that 67DHC chelated Fe2+ ions at pH 5.5, 6.8 and 7.5 at the chelating ratio 2:1...
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Copper reducing effects of flavones
Jeřábková, Markéta ; Karlíčková, Jana (advisor) ; Filipský, Tomáš (referee)
Charles University in Prague Faculty of Pharmacy in Hradci Králové Department of Pharmaceutical botanic and ecology Candidate: Mgr. Markéta Jeřábková Consultant: PharmDr. Jana Karlíčková, Ph.D. Title of Thesis: Copper reducing effects of flavones Free radicals are commonly present in our organism, however, in case of their accumulation it could cause many diseases. Copper is an important trace element which is essential for many biological processes. On the other hand, copper can catalyze processes which produce damaging radicals. Flavonoids are polyphenolic compounds with many biological effects. The most important is antioxidant activity which protects us from free radicals. Flavonids can also have a prooxidant effect. This thesis was focused on a detection of the reducing activity of flavones (mosloflavone, luteolin, apigenin, crysin, diosmin, 5-hydroxyflavone, baicalin, baicalein, negletein, apigenin-7-glucoside) at different pH. A reducing activity of surveyed flavones was taken by the methodics of spectrophotometric analysis with the use of a selective indicator of cuprous ionts formed in bathocuproinedisulfonic acid disodium salt at different pH. A reducing activity depends on the structure of flavones and pH environment. From the definition of the relation between the structure of a flavone...
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Analysis of oxidative stress in the model of isoprenaline carditoxicity after intravenous administration of rutinCardiovascular
Sedlářová, Lucie ; Filipský, Tomáš (advisor) ; Fikrová, Petra (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Pharmacology and Toxicology Candidate: Mgr. Lucie Sedlářová Supervisor: PharmDr. Tomáš Filipský, Ph.D. Title of thesis: Analysis of oxidative stress in the model of isoprenaline carditoxicity after intravenous administration of rutin Cardiovascular diseases are the leading cause of mortality in the developed countries. Among the most serious acute forms of ischemic heart disease belongs acute myocardial infarction (AMI), which can be caused by high levels of endogenous catecholamines. Isoprenaline (ISO), a synthetic catecholamine, evokes a pathological state similar to that of AIM, which is accompanied by an increase in both of unbound iron and copper and the consequent formation of hydroxyl radical in Fenton chemistry. Flavonoids are a large group of substances of natural origin, which represent an important component of human diet and are considered to be beneficial for health status. Their effects include free radical scavenging, iron/copper-chelating properties and inhibiting enzymes producing reactive oxygen species. However, several representatives have showed negative pro-oxidative effects as well. The main aim of this thesis was an analysis of oxidative stress in the model of isoprenaline cardiotoxicity...
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Oxidative Stress in the Model of Catecholamine Cardiotocitiy
Linhartová, Anna ; Filipský, Tomáš (advisor) ; Rathouská, Jana (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Pharmacology and Toxicology Candidate: Mgr. Anna Břečková Consultant: Mgr. Tomáš Filipský, Ph.D. Title of Thesis: Oxidative stress in the model of catecholamine cardiotoxicity Cardiovascular diseases are the world's most common cause of mortality and morbidity, in particular coronary heart disease and it's most severe form - acute myocardial infarction (AIM). Better prediction of AIM can be achieved by a detailed understanding of the mechanisms of its etiopatogenesis. In this study, we focused on the assessment of oxidative stress in 2-h model of isoprenaline cardiotoxicity, i.e. the acute state, which shares several pathophysiological similarities with early phase of AMI, in Wistar:Han rats. The marker of oxidative stress was glutathione. Moreover, the analysis of correlations of oxidized glutathione (GSSG), total glutathione (GSHt) and the ratio GSH/GSSG with ECG parametres was performed. The rats were divided into two groups, i.e. the control group (water for injections, 2 ml/kg, s.c.) and the isoprenaline group (isoprenaline, 100 mg/kg, s.c.). In rats, which were treated with isoprenaline and did not survive the 2-h experiment, a significant increase in the concentration of GSSG and decrease in ratio GSH/GSSG were...
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Copper chelating activity of flavonols
Jeřábková, Markéta ; Karlíčková, Jana (advisor) ; Filipský, Tomáš (referee)
Charles University in Prague Faculty of Pharmacy in Hradci Králové Department of Pharmaceutical botanic and ecology Candidate: Markéta Jeřábková Supervisor: PharmDr. Jana Karlíčková, Ph.D. Title of Thesis: Copper chelating activity of flavonols Copper belongs to essential trace elements. It is involved in different biological processses essential for life therefore metabolism disorders of copper can give rise to patological displays. A raised level of loose copper in serum at some diseases arouses a great interest in the "chelating" therapy and the study of new potential chelators. The importance of chelation is based on the maintenance of copper homeostasis and the elimination of its abundance. It serves the intoxication therapy of copper and other heavy metals and the treatment of Wilson's disease. Flavonoids are polyphenolic compounds with antioxidant effects. Flavonoids able to chelate some metal ions through which they reduce the possibility of the production of a hydroxyl radical which decrease the effect of oxidative stress on organism. The possible use of the "chelating" therapy with flavonoids is investigated also at cardiovascular and neurodegenerative diseases, the occurrence of cancer and the inflammation. This diploma thesis was focused on discovering chelating activity of flavonols:...
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Stanovení anthokyanidinů jako potenciálních ligandů lidského konstitutivního androstanového receptoru (hCAR) in vitro
Škoricová, Dagmar ; Pávek, Petr (advisor) ; Filipský, Tomáš (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Pharmacology and Toxicology Candidate: Mgr. Dagmar Škoricová Supervisors: Doc. PharmDr. Petr Pávek, Ph.D. Title of rigorosum thesis: Investigating of anthocyanidins as the putative ligands of the human constitutive androstane receptor (hCAR) in vitro Anthocyanidins are natural flavonoid compounds occurring in various fruits and berries, which represent an important part of the normal healthy diet. In addition to their doubtless health benefits, recent studies have suggested that flavonoids are able to activate xenosensors and therefore regulate a wide range of xenobiotic enzymes involved in the biotransformation of drugs, which might be associated with the increased risk of drug-food interaction. Human constitutive androstane receptor (hCAR) is a xenosensor and a nuclear receptor, which regulates the activity of various hepatic and extrahepatic biotransformation enzymes, especially from the CYP superfamily. In this thesis we used the molecular biology methods - Gene reporter assay and Two- hybrid assay to examine the ability of 6 diverse anthocyanidins, cyanidin, delphinidin, malvidin, pelargonidin, peonidin and petunidin to activate the hCAR receptor in vitro. We found, that none of the examined anthocyanidins has...
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Screening of Iron-chelating Substances and their Potential Use in the Therapy of Acute Myocardial Infarction
Filipský, Tomáš ; Hrdina, Radomír (advisor) ; Patočka, Jiří (referee) ; Štěrba, Martin (referee)
Charles University in Prague, Faculty of Pharmacy in Hradec Králové Department: Department of Pharmacology and Toxicology Candidate: Mgr. Tomáš Filipský First supervisor: prof. MUDr. Radomír Hrdina, CSc. Second supervisor: PharmDr. Přemysl Mladěnka, Ph.D. Title of doctoral thesis: Screening of iron-chelating substances and their potential use in the therapy of acute myocardial infarction Iron is an essential element virtually for all living organisms. The concentration of free/unbound iron is very low at physiological conditions. However, in several pathological states, its homeostasis is impaired which may lead to an organ damage due to the increased production of reactive oxygen species. Coronary heart disease is the main cause of morbidity and mortality worldwide. Its most serious form is acute myocardial infarction (AMI). During the early ischaemia, catalytically active elements, particularly iron and copper, are released into the blood circulation. After restoration of blood flow (reperfusion), these elements may participate in the production of biologically the most potent oxidant - hydroxyl radical via iron/copper catalysed Fenton reaction. Therefore, a therapy based on administration of iron/copper-chelating agents could be a potential pharmacotherapeutic approach in the treatment of this...
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Parasitostatus of red deer population in Eagle mountains (Czech Republic) a results of antiparasitic control
Filipský, Tomáš ; Lamka, Jiří (advisor) ; Ducháček, Lubomír (referee)
Thesis: Parasitostatus of red deer population in the Eagle Mountains (Czech Republic) and the results of antiparasitic control Made by: Tomáš Filipský The thesis deals with parasitostatus of red deer which is bred in the overwintering enclosures of the Eagle Mountains - Pádolí, Podlesí, Malá Strana. The thesis is aimed at qualitative and quantitative larvoscopic examination of individual anonymous samples of excrement and lungworm species Elaphostrongylus cervi, Varestrongylus sagittatus and Dictyocaulus viviparus. The parasitological examination showed only L1 larvae of Elaphostrongylus cervi the lungworm, the average prevalence of positive findings on the examination was 68.1 % in the winter season 2007/2008. The treatment effectivity was analysed in the overwintering enclosure Pádolí in the winter seasons 2007/2008 and 2008/2009. It achieved the value of 100.0 % in both seasons.
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