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Natural drugs in cancer treatment and their cytotoxicity
Hájková, Tereza ; Raudenská, Martina (referee) ; Provazník, Ivo (advisor)
The thesis deals with the natural substances in context with the cancer disease. The natural substances have a positive effect on the human organism and they are able to influence the viability and the growth of the cancer cells. The main mechanical device is to influence the mechanisms needed to start the apoptosis of the cancer cells and stopping further proliferation. The cancer cell lines utilization in the cancer disease is discussed in the thesis too. The thesis states common methods of determining the natural substances cytotoxicity. For the experimental part of the thesis it was chosen the MTT test method and the xCELLigence system for monitoring in real time. The mechanical device of the tested substance capsaicin in application on the prostate cell lines, tumorous PC3 and nontumorous PNT1A influence will be observed within the experimental part of the thesis.
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Study of natural substances of ginger
Dobiáš, Vojtěch ; Vespalcová, Milena (referee) ; Veselá, Mária (advisor)
The aim of this study was to determine the quantity of natural substances in ginger. Extracts from organic ginger tea and ginger rhizome were prepared using three different solvents. Antioxidant activity and the content of polyphenols and flavonoids were determined spectrophotometrically. Effects on bacterial growth of the extracts were studied against bacteria Bacillus cereus and Serratia marcescens by agar well diffusion assay. The obtained data showed, that there is a significant amount of difference between the contents of studied compounds in the two extract samples. The highest amount of polyphenols was found in ginger tea with concentration of 0,481 mgml-1, compared to 0,078 mgml-1 found in the ginger rhizome. The tea showed a greater antioxidant activity than the rhizome. Bacterial growth was slightly inhibited only by water extracts of the tea and this was only observed against Bacillus cereus.
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Natural compounds active against mycobacteria (review)
Kunáková, Martina ; Krátký, Martin (advisor) ; Vinšová, Jarmila (referee)
The main topic of the bachelor thesis is compounds isolated from natural sources, which contribute significantly to the discovery of new therapeutic methods in many medical problems. The aim of the work, was to focus specifically on those compounds that showed significant antimycobacterial activity against pathogens of the genus Mycobacterium, especially against M. tuberculosis. The theoretical part focuses on the genus Mycobacterium itself and its basic characteristics. In addition, the work also focused on the specific species causing the non-tuberculous forms of the disease and those behind the outbreak of tuberculosis in the human body. The last chapter of the theoretical part deals with tuberculosis and its brief description, together with the treatment and the issues related to development of drug resistance during treatment. In the following section, specific compounds that exhibit antimycobacterial activity and have the potential to be developed as new drugs are described. Keywords: aldehydes, alkaloids, antituberculotics, compounds of natural origin, cyanobacteria, essential oils, Mycobacterium tuberculosis, mycobacteria, naphthoquinones, resistance, steroid hormones, terpenes, triterpenes, tuberculosis
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Search for new natural alpha-glucosidase inhibitors
Kašpárková, Michaela ; Karlíčková, Jana (advisor) ; Carazo Fernández, Alejandro (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacognosy and Pharmaceutical Botany Student: Michaela Kašpárková Supervisor: PharmDr. Jana Karlíčková, Ph.D. Title of diploma thesis: Search for new natural α-glucosidase inhibitors α-glucosidase is one of the main enzymes that break down carbohydrates in the digestive tract. Its physiological function is mainly the cleavage of α-(1,4) bonds of oligosaccharides and enabling the absorption of D-glucose into the bloodstream. As a result, there is an increase in postprandial blood glucose values, which is not desirable in patients with diabetes or in people with a high risk of developing it. Flavonoids are natural polyphenolic substances found in many natural components of our food. These substances are known for their positive effects on human health, which also include the ability to inhibit the α-glucosidase enzyme. Therefore, the aim of this work was to determine the inhibitory activity of flavonoids against the α-glucosidase enzyme and the subsequent assessment of the structure-activity relationship. Using twenty-two selected flavonoids belonging to five different structural groups, the inhibitory activity on the yeast α-glucosidase from Saccharomyces cerevisiae was determined by spectrophotometric measurements in vitro....
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Phytochemical studies of potential phytopharmaceuticals using separation methods
Dulendarova, Elizabeta Hristiyanova ; Jenčo, Jaroslav (advisor) ; Křoustková, Jana (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department: Department of Pharmacognosy and Pharmaceutical Botany Candidate: Elizabeta Hristiyanova Dulendarova Supervisor: RNDr. Jaroslav Jenčo, Ph.D. Title of dissertation thesis: Phytochemical Studies of Potential Phytopharmaceuticals using Separation Methods The main aim of this diploma thesis was the identification of main alkaloidal components from the fraction of Papaver rhoeas L. (family Papaveraceae) alkaloidal extract - fraction PR-12-23. The introduction to the theoretical part summarizes alkaloids found in Papaver rhoeas L. and describes the separation methods used in the isolation process at the department of Phamacognosy and Pharmaceutical botany. Two main compounds within the extract were identified and separated based on HPTLC, HPLC-MS, and GC-MS chromatographic separation methods. For the subsequent fractions, the HPLC method development, optimization, and scaling up from analytical to preparative scale was done. After identification with the help of analytical HPLC and GC, the compounds were separated into fractions, isolated using preparative HPLC, and identified using NMR. The purified isolates were tested for anti-butyrylcholinesterase and cytotoxic biological activity, linked to AD and cancer, respectively. The first...
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Conjugate Addition Coupled with Enolate Oxidation in the Total Synthesis of Natural Polyphenols
Mašek, Tomáš ; Jahn, Ullrich (advisor) ; Pospíšil, Jiří (referee) ; Švenda, Jakub (referee)
1 ABSTRACT This thesis describes the development of the concept of C-C bond forming conjugate addition/oxidative cyclisation reactions and their application in the total synthesis of natural polyphenols. The first part deals with the development of methodology for conjugate addition of main- group organometallic reagents to unsaturated carbonyl compounds coupled with in situ single electron transfer oxidation. The resulting radical undergoes stereoselective cyclisation, that can be followed by a second SET oxidation, leading to further cationic cyclisation. This methodology is ideally suited for the synthesis of furoindane stilbenolignans (FIS), a neglected and structurally distinct class of natural polyphenols. Using this process, racemic synthesis of a derivative of kompasinol A was achieved, confirming the relative configuration of FISs. In an effort to develop asymmetric route to FISs, an unprecedented direct conjugate addition of aryllithiums to ylidenemalonates mediated by diethers and diamines was discovered, leading to asymmetric synthesis of gnetifolin F and 11- deoxykompasinol A. Based on X-ray evidence, a related annulation methodology consisting of direct conjugate addition/epoxide opening was shown to result in bridged lactones, instead of isomeric FISs. This finding led to an approach for the...
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Biological activity evaluation of substances of natural origin I.
Kupčíková, Júlia ; Suchánková, Daniela (advisor) ; Kučera, Tomáš (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacognosy and Pharmaceutical botany Candidate: Júlia Kupčíková Supervisor: PharmDr. Daniela Suchánková, Ph.D. Title of diploma thesis: Biological activity evaluation of substances of natural origin I. Alzheimer's disease (AD) is progressive neurodegenerative brain disorder characterized by memory loss and cognitive impairments. Manifestation of this disease is associated with decreased level of acetylcholine. Current treatment of AD is symptomatic and involves mainly restoring of acetylcholine levels through cholinesterase inhibition. Galanthamine, one of acetylcholinesterase inhibitors indicated for the treatment of AD belongs to Amaryllidaceae alkaloids. Therefore, other Amaryllidaceae alkaloids and their derivatives are prepared and studied for similar inhibitory properties. Amaryllidaceae alkaloid vittatine does not have cholinesterase inhibitory properties, but previous findings proved that some vittatine derivatives have potency to inhibit both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). Seven new semisynthetic derivatives of vittatine were prepared and studied for their inhibitory potential against both cholinesterases, using the Ellman's method. Significant BuChE inhibitory activity was...
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Using tandem cyclisation/Sonogashira cross-coupling in the synthesis of natural products and their derivatives
Liška, Benno ; Matoušová, Eliška (advisor) ; Míšek, Jiří (referee)
The subject of this bachelor's thesis is the preparation of polycyclic compounds using the tandem cyclisation/Sonogashira cross-coupling and a potential application of this reaction to the synthesis of natural products and their derivatives. The aim was to study this method using nonaromatic starting materials with a six-membered ring and to explore possibilities for functionalisation of the triple bond of the newly prepared compounds. The first part of this thesis deals with the synthesis of starting materials containing either an ether group or a malonate residue. The second part deals with the optimisation of conditions and the investigation of the scope of Heck reaction and Sonogashira cross-coupling. The third part describes the attempts to hydrate the triple bond and the last part contains reactions with allylic alcohols. Keywords: synthesis, tandem reaction, natural products, Sonogashira cross-coupling, Heck reaction
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Drugs used in clinical practice with the origin in plants
Šímová, Markéta ; Suchánková, Daniela (advisor) ; Pourová, Jana (referee)
Charles Univerzity, Faculty of Pharmacy in Hradec Králové Department: Department of Pharmacognosy and Pharmaceutical botany Author: Markéta Šímová Supervisor: PharmDr. Daniela Hulcová Ph.D. Title of thesis: Active substances used in clinical practice originating in plant sources Key words: active substance, plant source, development, analgesics, local anesthetics, antineoplastics, sympathomimetics, parasympathomimetics, parasympatholytics, antispasmodics. Since time immemorial, plants have been used to treat various diseases, but it is not known what is behind their healing effect. It managed to find out with the development of pharmacy and chemistry. The first substances were isolated and their mechanism of action was elucidated. It was found that the substances themselves have a better and more efficient effect than the mixture, but also a number of side effects. The effort of experts was to remove them, which managed to prepare a lot of derivatives and in many cases they had even higher effect. With the development of new technologies, synthetically produced substances have come to the fore and it is already forgotten that many clinically used drugs have their origins in nature. This thesis deals with substances that originate in plant sources and are used in clinical practice as medicinal...
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Natural drugs in the treatment of productive cough
Čontofalská, Natália ; Pourová, Jana (advisor) ; Karlíčková, Jana (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacology & Toxicology Student: Natália Čontofalská Supervisor: doc. PharmDr. Jana Pourová, Ph.D. Title of diploma thesis: Natural drugs in the treatment of productive cough Cough is a physiological defensive reflex and it is also a symptom of many acute or chronic diseases. Cough can be categorized as dry irritant or productive. Productive cough can be treated by conventional drugs and medicinal plants. Medicinal plants contain various types of chemicals and some of them have expectorant properties. Chemical constituents are commonly members of saponin, flavonoid or essential oil groups. This diploma thesis presents summary of the most important results and information from literature, pharmacological experiments and clinical studies confirming their efficiancy. Some of the articles provide explanation of mechanism of action of the chemicals with expectorant properties. Other effects of these plants may also contribute to the therapeutic effect.
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