|
Pyridine sulphides as antituberculotic active compounds
Sýkora, Lukáš ; Kuneš, Jiří (referee) ; Klimešová, Věra (advisor)
This diploma thesis is devoted to antituberculosis drugs research. A very briefly depicts of genus Mycobacterium, structure and composition of mycobacterial cell wall allowed here better process and determination of mechanisms of antituberculosis drugs targets. The synthesis selected derivates of pyridine sulfides: 4- (phenethylsulfanyl)pyridine-2-carbonitriles are the main aim of the diploma thesis. As well as a possible mechanism of action these substances is discussed. Thus a series of 4-(phenethylsulfanyl)pyridine-2-carbonitriles were synthesized. The structures were confirmed by IR spectra, NMR spectra and elementary analyses. Antimycobacterial activities these compounds were tested against Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium kansasii. None of prepared substances exhibited activity (against M. tuberculosis) comparable to clinical used antituberculosis drugs. Significant activity was observed (in compare with isoniazide) against M. kansasii and M. avium.
|
|
Ecotoxicological study of the select drug
Střílková, Dagmar ; Vytlačilová, Jitka (referee) ; Vytlačilová, Jitka (advisor)
Dagmar Střílková, Ecotoxicologial study of the select drug, diploma work Charles University in Prague, Faculty of Pharmacy, Department of Pharmaceutical Botany and Ecology Ibuprofen, the effective substance of drug IBALGIN® 400 mg, belongs to widely used nonsteroidal antiinflammatory drugs. It is primary used to treat most of the inflammatory illnesses. The renal excreting is the most important way of the final elimination. Ibuprofen can get into surface, ground and drinking water. Because of the interpretation of the result for impact on enviroment, the acute toxicity of this pharmaceutical was evaluated on organism of all the trophic levels. The green alga S capricornutum was chosen like the representative of the procedurs, which is used in 72 hour growth inhibition test ALGALTOXKIT F. Crustacean T platyurus of the series of the consumers was used in 2 next tests. The mortality of the larva of this crustacean is found out by means of 24 hour test THAMNOTOXKIT F. RAPIDTOXKIT evaluates the inhibition of the food receiving by the crustacean. 2 tests were done on the representative of the decomposer, T pyriformis. PROTOXKIT F evaluates the growth inhibition of this ciliate. MTT bioassay is based on the reduction of tetrazolium salt (MTT) by the mitochondrial dehydrogenace of viable cells in formazan....
|
|
Importance of Transporter Proteins for Fetal Protection
Hahnová, Lenka ; Štaud, František (advisor) ; Anzenbacher, Pavel (referee) ; Geršl, Vladimír (referee)
Doctoral thesis Mgr. Lenka Hahnová (Cygalová) Placenta, which represents a unique link between the mother and fetus, fulfills many functions essential for normal course of pregnancy and uncomplicated development of the fetus. Nutrient supply, gas exchange and metabolic waste product removal belong to its main roles. In addition, placenta serves as an endocrine, metabolic, immune and protective organ, since during pregnancy mother may be, either unconsciously or deliberately, exposed to a wide range of substances toxic for the fetus. Originally, it was supposed that the physiological barrier between maternal and fetal circulation is created only by cellular layers of syncytiotrophoblast and endothelium of fetal capillaries. However, it has been demonstrated that besides this mechanical component of protection, activity of drug efflux transporters and metabolic enzymes localized in the polarized syncytiotrophoblast layer contribute considerably to the protective function of placental barrier. Efflux transporters are ATP dependent membrane proteins capable of actively removing different molecules out of cells. So far, the best described drug efflux transporters are P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP), significantly affecting kinetics of transplacental passage of various...
|
|
Extracellular space diffusion parameters and metabolism in the rat somatosrensory cortex during recovery from trabsient global ischemia and hypoxia
Zoremba, Norbert ; Syková, Eva (advisor) ; Mareš, Pavel (referee) ; Rokyta, Richard (referee)
Content Abstract .................................................................. ..... ...... ............................ .... 2 Introduction ............................................ ........................................ .................. 4 Aims .................. ................. ................................ ....... ..... . ............ .......... 6 Methods ............................................... ......................................................... ... 7 Results ................ ............................................................................ .................. 9 Discussion .. ... ............... .. ......... .. .......................... ............................. ... ............. 13 References ....... ................................................................ ....................... ........ 20 List of Publications ............. .... .. ............... .. ... .. .......... .. ... ............................... .... 22 Abstract The extracellular space (ECS) of the brain represents the microenvironment of nerve cells and enables the diffusion of neuroactive substances among neurons, axons and glia. Changes in the ECS diffusion parameters during ischemia are well known, but information about changes in ECS diffusion and energy-related metabolite...
|
|
Influence of Cholestatic Liver Injury on the Elimination and Transport of Drugs
Brčáková, Eva ; Štaud, František (advisor) ; Tilšer, Ivan (referee) ; Lotková, Halka (referee)
The liver is a unique organ with a number of vital functions. Pivotal one is its participation on bile formation and secretion, import, detoxification and excretion of endogenous substances and xenobiotics. Bile formation is essential for both absorption of lipids in intestine and excretion of various endogenous compounds and xenobiotics (e.g. bile acids, bilirubin, cholesterol, phospholipids and drugs). This function is markedly impaired during extrahepatic and intrahepatic cholestasis with partial or complete stoppage of bile flow. Consequently, hepatic and further systemic accumulation of toxic biliary constituents, such as bile acids and bilirubin, occurs. In an effort to compensate this situation, spontaneous anti-cholestatic mechanisms are activated, which provide alternative excretory routes for toxic accumulating compounds (e.g. renal elimination of bile acids and xenobiotics into urine). These mechanisms include changes in the expression, localization and function of respective transporters in liver and kidneys. Another mechanism with a significant impact on bile formation and transport of compounds between bile and blood is blood-biliary barrier formed by connection of hepatocytes by "tight-junctions" and "gap-junctions". While "gap-junctions" exchange substances among cells,...
|
|
Rights of a child under the competence of bodies responsible for social and legal protection of children
Sabolová, Zuzana ; Radvanová, Senta (advisor) ; Dvořák, Jan (referee)
70 Resumé In my thesis named " Rights of a child within the scope of the social-legal child protection authorities" I tried to focus on the activity of different entities relating to the social-legal protection of children. I have chosen this theme because I think this problem is very important and each advanced society should protect and take care of children as they can't take care of themselves. The thesis provides an initial introduction to the statutory regulations relating to the social-legal protection of children, which are primarily set out in Act No. 359/1999 Sb., on social-legal protection of children. In the present work I offer a brief overview of the most important child protection institutes, with focusing on the specific activity of the public authorities and the private entities operating in this area. My thesis is conceptually devided into seven, logically linked chapters in which I am trying to demonstrate the protection of children. In the first chapter there is a brief overview of the historical evolution of the social-legal protection of children, then, in the second chapter I am mentioning the most important law sources relating to the delineated issue. In the third chapter I tried to define the family as a basic social cell and its importance for children. The fourth and the fifth...
|
|
Nursing process procedure in patient with an injury of cervical spine
Juzová, Lucie ; Nikodemová, Hana (advisor) ; Nesnídal, Petr (referee)
I wrote my bachalor's work about Nursing treatment of patient with injury of cervical spine. The work is divided into theoretical and practical part. I directed the theoretical part to anatomy and biomechanics of spine and spinal cord, to etiology, symptoms and classification of injury of cervical spine. Then I paid attention to principles of first aid and mainly to diagnostic and treatment. I mentioned prevention and prognosis of this disease. ln the practical part I paid attention to nursing treatment of particular patient with injury of cervical spine and transversal spinal lesion. I took care about this patient in the spondylosurgery ward, where the transfusion of the stem cells was made to him. During the hospitalization I to ok nursing anamnesis according to Majory Gordon and I set nursing diagnosis and their aim. I drew up a pIan of treatment, which I realized and than I evaluated the result of provided treatment. In one part I paid attention to education of patient. At the end I described how I took steps during writting my work, if my method of treatment came right and I informed about my knowledge and experiences. I included the medical dokumentation and some topical pictures to the appendix. Powered by TCPDF (www.tcpdf.org)
|
|
Dysfunction of Endothelium in Relationship to Experimentally Induced
Černý, Dalibor ; Nachtigal, Petr (advisor) ; Štaud, František (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Biological and Medical Sciences Rigorous Thesis - Abstract Name: Mgr. Dalibor Černý Year: 2007 Dysfunction of Endothelium in Relationship to Experimentally Induced Anthracycline Drugs' Toxicity Endothelial dysfunction is defined as functional lesion of endothelium, characterized by increased permeability of vessel wall, by imbalance among vasoactive, coagulative and proliferation influencing active substances, in result leading to increased expression of cell adhesion molecules VCAM-1 and ICAM-1, which are considered as standard morphological markers of its progress. Adhesion molecules VCAM-1 and ICAM-1 play an important role in building-up of inflammatory reaction and take part in various pathological stages. They are expressed by endothelial cells, by scavenger cells, macrophages and smooth muscle cells. The aim of this rigorous thesis was to examine whether long-lasting daunorubicin administration leads except of significant changes in heart also to the progress of endothelial dysfunction. Imunohistochemical methods were used to detect the expression of these adhesion molecules. Then, the selected heart parameters like LVEF (left ventriculum eject fraction), FS (fractional shortening) and dP/dtmax index, that means peak...
|
|
Studies on NKR-P1A and NKR-P1B receptors expressed in eukaryotic organisms
Ivanova, Lyubina ; Rychlovský, Petr (referee) ; Bezouška, Karel (advisor)
NK (natural killer) cells, with their ability to identify antigens and extraneous substances, available in the organism through various moleculary receptors, are an important component of the immune system. The NKR-P1A and NKR-P1B proteins belong to the lectin receptors of natural killer cells. Primary ligands of lectin receptors comprise terminal oligosaccharides of glycoproteins on the surface of target (e.g. tumor) cells. The interaction between carbohydrate structures on the surface of antigens and their binding partners on NK receptors is followed by triggering the effector function of NK cells against the targets. The NK cells and NK receptors findings and their interactions with ligands are greatly utilized in the treatment of cancer, viral and autoimmune diseases. Heterologous protein production in the eukaryotic organism brings a lot of advantages. Unlike the prokaryotic organism, the methylotrophic yeast Pichia pastoris has the capability of performing many posttranslational modifications resulting in production of biological active protein molecule. Usually, the P. pastoris expression system disposes of high level protein expression and is also generally regarded as being faster, easier, and less expensive to use than expression systems derived from other eukaryotes. In this thesis, I...
|
|
Small signaling molecules in yeast
Putalová, Tereza ; Váchová, Libuše (advisor) ; Horníková, Lenka (referee)
Yeasts excrete metabolitesinto the environment some of which may have a signal function. The small signalling molecules include ammonia, alcohols, esters, acids and CO2 beside other molecules. These substances may be formed as waste products of metabolism, such as some alcohols in the catabolism of amino acids. After exclusion they influence other / surrounding cells by binding to receptors or they affect their target in the cell or may form a concentration gradient or a pH gradient. New findings show that using ammonia yeasts can communicate and may diversify within colonies. Farnesol, tyrosol and other molecules use the yeasts to quorum sensing. Yeasts also secrete aromatic esters and fatty acids. High concentrations of CO2 trigger switch from yeasts to hypha. This paper summarizes existing information on the occurrence and impact of selected molecules (ammonia, alcohols, esters, acids and CO2) signaling in the yeast Saccharomyces cerevisiae and Candida albicans.
|
guest ::
