National Repository of Grey Literature 201 records found  beginprevious112 - 121nextend  jump to record: Search took 0.00 seconds. 
Elimination of alcohol in blood of patients treated with coumarin drugs
Kahounová, Jana ; Vopršalová, Marie (advisor) ; Trejtnar, František (referee)
CHARLES UNIVERSITY Faculty of Pharmacy in Hradec Králové Department of Pharmacology & Toxicology Student: Jana Kahounová Supervizor: Doc. PharmDr. Marie Vopršálová, Ph.D. Ing. Jaroslav Procházka Title of diploma thesis: ELIMINATION OF ALKOHOL IN BLOOD OF PATIENTS TREATED WITH COUMARIN DRUGS Coumarin preparations are the most commonly used oral anticoagulants. The main representative is Warfarin. The most important function of warfarin is to reduce the formation of K-dependent coagulation factors in the liver. Alcohol is the oldest and most widely used addictive substance. Alcohol is the oldest and most commonly used substance. Society is tolerated and regular use of small doses of alcohol is considered "beneficial to health". The aim of my thesis was to find out how the concomitant use of coumarin drugs and alcohol interacts. There were tested 62 people (33 men and 29 women), of whom 27 people (14 men and 13 women) were treated with coumarin drugs, 35 people (19 men and 16 women) formed the control group of individuals without treatment with coumarin drugs. All people were given a standard dose of alcohol. The blood alcohol level (COBAS INTEGRA 400 plus) and INR (SYSMEX CA 1500) were measured in the time-0 (before administration), 1½ and 3 hours (after administration). The data obtained was...
In vitro evaluation of novel Toll-like receptor ligands II.
Machalová, Vanda ; Trejtnar, František (advisor) ; Janočková, Jana (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology & Toxicology Student: Vanda Machalová Supervisor: doc. PharmDr. František Trejtnar, CSc. Title of diploma thesis: In vitro evaluation of novel Toll-like receptor ligands II. The aim of this diploma thesis was to test the new substances at Toll-like receptors (TLR), namely TLR4 and TLR8 subtypes, as potential vaccine adjuvants. Adjuvants are required for new subunit vaccines to promote stimulation of a sufficient immune response. Stimulation of TLR receptors is safe and leads to the activation of both innate and adaptive immunity and to subsequent specific immune response. Testing was carried out on cell lines stable co-expressing the respective receptors, with colorimetric activity detection. In this work, both agonist and antagonist activity at TLR4 and TLR8 receptors was investigated and a half maximal effective concentration (EC50) of resiquimod was determined. Based on the results, the respective substances cannot be considered as potential adjuvants to the TLR8 receptor and DM014 exhibits the potential for agonist activity on the TLR4 receptor, whereas the substance DM015 can be used on further investigation of immunosuppression in autoimmune diseases and diseases associated with excessive activation of the...
In vitro evaluation of novel Toll-like receptor ligands I.
Hudáková, Kristína ; Trejtnar, František (advisor) ; Soukup, Ondřej (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology and Toxicology Student: Kristína Hudáková Supervisor: doc. PharmDr. František Trejtnar, CSc. Title of diploma thesis: In vitro evaluation of novel Toll-like receptor ligands I Vaccination against preventable infections prevents millions of deaths each year. Their immunity enhancing activity is strengthened by the presence of vaccine adjuvants. Development of vaccine adjuvants leads to improved safety profile and also can play a vital role in the research of new vaccines against pathogens against which the vaccines currently do not exist. The main aim of this diploma thesis was to verify the ability of rationally developed small molecule ligands to influence Toll-like receptors and thus their potential to be utilized as vaccine adjuvants. The assay was carried out using modified cell lines continually expressing the human TLR4 or TLR8 whose activation leads to production of secreted embryonic alkaline phosphatase. Ten analyzed substances labelled as DM 001 - DM 010 were examined for their agonistic and also antagonistic properties while interacting with the TLRs. Immunomodulatory activity of these tested samples was then determined by quantification of secreted alkaline phosphatase with the help of a colorimetric...
Modulation of biotransformation and antioxidant enzymes by selected natural compounds
Lněničková, Kateřina ; Szotáková, Barbora (advisor) ; Anzenbacherová, Eva (referee) ; Trejtnar, František (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences Candidate: Mgr. Kateřina LNĚNIČKOVÁ Supervisor: prof. Ing. Barbora SZOTÁKOVÁ, Ph.D. Title of Doctoral Thesis: MODULATION OF BIOTRANSFORMATION AND ANTIOXIDANT ENZYMES BY SELECTED NATURAL COMPOUNDS Public interest in various dietary supplements containing herbs, herbal extracts or isolated active compounds has increased significantly over past decades. Consumption of these supplements increases worldwide and they are often consumed in unreasonably high doses, as they are generally considered as safe. Upon the intake to organism, these compounds are, as other xenobiotics, modified mostly by xenobiotic-metabolizing enzymes and they could influence these enzymes at the same time. Potential modulation of xenobiotic-metabolizing enzymes' activity (induction or inhibition) can seriously affect pharmacokinetics of concomitantly administered drugs. Knowledge of the possible impact of natural compounds on the xenobiotic-metabolizing enzymes is essential for their safe use. The aim of this doctoral thesis was to study the effects of selected herbal extracts and their active chemical constituents on the activity and expression of xenobiotic-metabolizing and antioxidant enzymes. We have focused on the study of effects of...
Detection of epithelial-mesenchymal transition markers (EMT) in cells in vitro
Špaček, Petr ; Szotáková, Barbora (advisor) ; Trejtnar, František (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences Candidate: Petr Špaček Supervisor: Doc. Ing. Barbora Szotáková, Ph.D. Consultant: RNDr. Věra Králová, Ph.D. Title of diploma thesis: Detection of epithelial-mesenchymal transition (EMT) markers in cells in vitro Epithelial-mesenchymal transition (EMT) is a process during which motile mesenchymal-like cells develop from non-motile parent epithelial cells. Physiologically, EMT plays important roles during embryonic development and wound healing. Loss of control over this mechanism can lead to fibrosis and cancer progression. Motile mesenchymal-like cells can pass through the basal lamina, get into the blood vessels and spread to distant tissues. Transition is regulated by EMT biomarkers. The biomarkers comprise wide spectrum of proteins, including cell surface proteins (E-cadherin, N-cadherin), cytoskeletal proteins (vimentin), microRNA (miR 200) and transcription factors (Snail, Twist). In this study, expression of EMT biomarkers was evaluated using RT-PCR and Western blotting. The ability to migrate was assessed using real-time analysis with the x-CELLigence system. Two known triggers of EMT, the StemXVivo™ EMT Inducing Media Supplement (IS) and TGF-β, were compared in human oral cancer cell lines DOK and...
Interactions of antiretrovirals with drug efflux transporters and their role in the transplacental pharmacokinetics
Ptáčková, Zuzana ; Štaud, František (advisor) ; Trejtnar, František (referee) ; Ulčová-Gallová, Zdeňka (referee)
Charles University in Prague, Faculty of Pharmacy in Hradec Králové Department of Pharmacology and Toxicology Candidate: Mgr. Zuzana Ptáčková Supervisor: prof. PharmDr. František Štaud, Ph.D. Consultant: PharmDr. Lukáš Červený, Ph.D. Title of doctoral thesis: Interactions of antiretrovirals with drug efflux transporters and their role in the transplacental pharmacokinetics The combination antiretroviral therapy that should be administered during the whole pregnancy is the backbone of prevention of mother-to-child transmission of HIV infection. One of the prophylactic mechanisms of such treatment is the presence of antiretrovirals in the fetal circulation. However this can be associated with the potentially harmful effects of drugs on the developing fetus. To select optimal therapy while minimizing risks it is inevitable to have detailed knowledge of all the factors affecting transplacental transport of drugs. The aim of this study was to detect whether drug efflux transporters are able to protect fetus against xenobiotics can affect the transplacental pharmacokinetics of the selected antiretroviral drugs. Employing variety of in vitro, in vivo, in situ and ex vivo methods we determined the role of the drug efflux transporters in the distribution of drugs between mother and fetus. We suggested that...
Mechanisms of membrane transport of radiolabeled receptor-specific peptides in the kidney
Volková, Marie ; Trejtnar, František (advisor) ; Mičuda, Stanislav (referee) ; Komárek, Pavel (referee)
Charles University in Prague, Faculty of Pharmacy in Hradec Králové Department of Pharmacology and Toxicology Candidate: PharmDr. Marie Volková Supervisor: doc. PharmDr. František Trejtnar, CSc. Title of doctoral thesis: Mechanisms of membrane transport of radiolabeled receptor-specific peptides in the kidney Radiolabelled receptor-specific peptides are a useful tool for radiodiagnostic and radiotherapy of some neuroendocrine tumours. Despite many recent developments in this radiopharmaceutical group, there is still a lack of relevant information about the mechanisms determining the pharmacokinetics and describing interactions with membrane transport systems. These transporters may be responsible for undesirable renal accumulation and subsequent radiotoxic kidney damage, which significantly limited the use of radiopeptides in nuclear medicine. The aim of our work was to assess the role of several transport mechanisms that can be potentially involved in the transmembrane transport of radiopeptides in the renal tissue. We mainly focused on studying the role of megalin mediated active endocytosis, fluid phase endocytosis and important human renal SLC transporters - hOAT1 and hOCT2. Simultaneously, the potential transport of selected radiometabolites of these peptides was studied in vitro and their...
Interactions of antiretrovirals with drug efflux transporters and their role in the transplacental pharmacokinetics
Ptáčková, Zuzana ; Štaud, František (advisor) ; Trejtnar, František (referee) ; Ulčová-Gallová, Zdeňka (referee)
Charles University in Prague, Faculty of Pharmacy in Hradec Králové Department of Pharmacology and Toxicology Candidate: Mgr. Zuzana Ptáčková Supervisor: prof. PharmDr. František Štaud, Ph.D. Consultant: PharmDr. Lukáš Červený, Ph.D. Title of doctoral thesis: Interactions of antiretrovirals with drug efflux transporters and their role in the transplacental pharmacokinetics The combination antiretroviral therapy that should be administered during the whole pregnancy is the backbone of prevention of mother-to-child transmission of HIV infection. One of the prophylactic mechanisms of such treatment is the presence of antiretrovirals in the fetal circulation. However this can be associated with the potentially harmful effects of drugs on the developing fetus. To select optimal therapy while minimizing risks it is inevitable to have detailed knowledge of all the factors affecting transplacental transport of drugs. The aim of this study was to detect whether drug efflux transporters are able to protect fetus against xenobiotics can affect the transplacental pharmacokinetics of the selected antiretroviral drugs. Employing variety of in vitro, in vivo, in situ and ex vivo methods we determined the role of the drug efflux transporters in the distribution of drugs between mother and fetus. We suggested that...
Effect of Synthetic Magnolol Derivatives on Activity of Nuclear Receptors PPARγ and RXRα
Dymáková, Andrea ; Szotáková, Barbora (advisor) ; Trejtnar, František (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences University of Vienna Faculty of Life Sciences Department of Pharmacognosy Candidate: Andrea Dymáková Supervisors: Mag. Simone Latkolik, doc. Ing. Barbora Szotáková, Ph. D. Title of diploma thesis: Effect of Synthetic Magnolol Derivatives on Activity of Nuclear Receptors PPARγ and RXRα The nuclear receptors, peroxisome proliferator-activated receptor γ (PPARγ) and its heterodimerization partner retinoid X receptor α (RXRα) are drug targets in the treatment of diseases like the metabolic syndrome and diabetes mellitus type 2. The effort has been made to develop new agonists for PPARγ to obtain ligands with more favourable properties than currently used drugs (Berger et al. 2002, Berger et al. 2005). Magnolol was previously described as a dual agonist of PPARγ and RXRα (Fakhrudin et al. 2010, Zhang et al. 2011). Based on the bi- aryl structure of magnolol, the effort has been made to design and synthesize linked magnolol dimers. The aim of this thesis was to investigate the agonistic potential of these compounds with respect of the nuclear receptors PPARγ and RXRα in comparison to magnolol. We evaluated the ligand binding properties of the compounds and their functionality as PPARγ agonists in vitro...

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