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Derivatives of Amaryllidaceae alkaloids and their biological activitydisease
Potůčková, Adéla ; Cahlíková, Lucie (advisor) ; Kuneš, Jiří (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Botany Candidate: Adéla Potůčková Supervisor: doc. Ing. Lucie Cahlíková, Ph.D. Title of diploma thesis: Derivatives of Amaryllidaceae alkaloids and their biological activity The plants of Amaryllidaceae family are source of a large amount of biologically active substances called Amaryllidaceae alkaloids. Their effects include cytotoxic, antifungal, antiviral, antibacterial or antimalaric activity and, last but not least, the inhibition of cholinesterases. The Amaryllidaceae alkaloids, galanthamine type also includes alkaloid chlidanthine, which is a positional isomer of the clinically practice used alkaloid galanthamine. The sources of chidanthine are Chlidanthus fragrans, Haemanthus multilflorus and Hippeastrum aulicum. The object of this thesis was the preparation of chlidanthine derivatives, and the study of their biological activity connected to the therapy of Alzheimer's disease and cancer. Ten aromatic ester derivatives of chlidanthine were prepared. The chemical structures were elucidated by NMR, MS experiments and optical rotation. Most derivatives were screened for their AChE and BuChE inhibitory potential and their cytotoxic potential against a panel of tumor and non-tumor cell lines. The most...
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Derivatives of Amaryllidaceae alkaloids and their biological activity: Derivatives of tazettine I
Pidaný, Filip ; Cahlíková, Lucie (advisor) ; Kuneš, Jiří (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Botany Candidate: Filip Pidaný Supervisor: Assoc. Prof. Ing. Lucie Cahlíková, Ph.D. Title of diploma thesis: Derivatives of Amaryllidaceae alkaloids and their their biological activity: Derivatives of tazettine I A study conducted between 1981 and 2014 found that 65% of small molecule based drugs are related to natural substances. The plants of the family Amaryllidaceae contain a particular and still not fully investigated group of alkaloids called Amaryllidaceae alkaloids. Their important biological effects include, for example, antiviral, antibacterial, antifungal, antiparasitic, cytotoxic and, in particular, motor-neuronal system-mediated effects mediated by inhibition of cholinesterases. A widespread Amaryllidaceae alkaloid is tazettine, a structural type alkaloid of tazettine that has increased interest in the early 1970s due to its cytotoxic acitivity, but appears less interesting in the studies conducted. The subject of this thesis was the preparation of tazettin alkaloid derivatives. The cholinesterase inhibitory activity was then tested. Cytotoxic activity in a panel of selected tumor and healthy cell lines was studied by screening. Unfortunately, none of the derivatives prepared by us showed an...
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Derivatives of Amaryllidaceae alkaloids and their biological activitydisease
Potůčková, Adéla ; Cahlíková, Lucie (advisor) ; Kuneš, Jiří (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Botany Candidate: Adéla Potůčková Supervisor: doc. Ing. Lucie Cahlíková, Ph.D. Title of diploma thesis: Derivatives of Amaryllidaceae alkaloids and their biological activity The plants of Amaryllidaceae family are source of a large amount of biologically active substances called Amaryllidaceae alkaloids. Their effects include cytotoxic, antifungal, antiviral, antibacterial or antimalaric activity and, last but not least, the inhibition of cholinesterases. The Amaryllidaceae alkaloids, galanthamine type also includes alkaloid chlidanthine, which is a positional isomer of the clinically practice used alkaloid galanthamine. The sources of chidanthine are Chlidanthus fragrans, Haemanthus multilflorus and Hippeastrum aulicum. The object of this thesis was the preparation of chlidanthine derivatives, and the study of their biological activity connected to the therapy of Alzheimer's disease and cancer. Ten aromatic ester derivatives of chlidanthine were prepared. The chemical structures were elucidated by NMR, MS experiments and optical rotation. Most derivatives were screened for their AChE and BuChE inhibitory potential and their cytotoxic potential against a panel of tumor and non-tumor cell lines. The most...
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Derivatives of Amaryllidaceae alkaloids as drugs
Ritomská, Aneta ; Cahlíková, Lucie (advisor) ; Kučerová, Marta (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Botany Candidate: Aneta Ritomská Supervisor: Assoc. Prof. Ing. Lucie Cahlíková, Ph.D. Title of diploma thesis: Derivatives of Amaryllidaceae Alkaloids as Drugs Plants of the family Amaryllidaceae belong to the widespread species. They contain a large amount of Amaryllidaceae alkaloids (AA) which are known for their biological activity. AA possess a broad spectrum of biological activities including an antiviral, antimalarial, antitumor, cholinesterase's inhibitory activity and others. An interesting AA is ambelline which occurs mainly in plants of the genus Crinum and Nerine. So far the biological activity of this compound has been studied only marginally. In the studies conducted, this substance appears to be less interesting. A series of aliphatic and aromatic derivatives of ambelline has been prepared in the framework of this thesis. Subsequently, their cholinesterase inhibitory activity and GSK-3β inhibitory activity were studied. Cytotoxic activity on a panel of selected tumor and resting cell lines was also screened. Of the prepared derivatives, LC-125 (3-methoxybenzoylambellin) had an interesting biological activity. This substance showed a promising activity in all biological studies. GSK-3β inhibitory...
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The legal nature of financial derivatives under Czech law
Kofroň, Jan ; Kohajda, Michael (advisor) ; Kotáb, Petr (referee)
The thesis deals with the analysis focusedm on the nature of financial derivatives based on the analysis of documents such as mainly academic literature and the relevant legal regulations. This thesis is focused on the Czech legal regulation of derivatives and also includes the relevant European legislation. Firstly, attention is aimed at derivatives in general, the first chapter is focused on a brief historical development in the field of derivatives, and than on the term derivatives itself, as explained by various authors and, for comparison, some international organizations. Subsequent chapter acquaints with the basic properties of derivatives, where the individual types are characterized - especially forwards, futures, swaps and options. The chapter concludes with the current state of the derivatives market. The following chapter deals with the regulation of derivatives and derivatives markets under the Czech and the European law. Firstly, the role and competence of the Czech National Bank as the central administrative authority with the powers of the regulatory body and the financial market supervisory authority in the Czech Republic is mentioned here for the purpose of underlying the complexity of the topic. Subsequently, it is followed by description of regulatory steps made by the European...
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Synthesis of haemanthaminy derivatives and their biological activity
Bodoríková, Viera ; Cahlíková, Lucie (advisor) ; Kučerová, Marta (referee)
4 ABSTRACT Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Botany Candidate: Viera Bodoríková Supervisor: doc. Ing. Lucie Cahlíková, Ph.D. Title of Diploma thesis: Synthesis of haemanthamine derivatives and their biological activity Haemanthamine, an isoquinoline Amarillidaceae alkaloid, exhibits a wide and important range of biological activities, including antitumor, antiviral, antioxidant, antimalarial and anticonvulsant. Biological activity of haemanthamine relatives closely with its structure. By modifying the different parts of the molecule, we can identify some structure-activity relationships. With this aim, the thirteen semisynthetic analogues of alkaloid haemathamine were prepared and purified using analytic and preparative TLC methods. The obtained substances were then subjected to structural analysis, specifically, there were used MS, HRMS, 1D and 2D NMR spectroscopic techniques. Prepared compounds were tested on its possibility to inhibit human erythrocytic acetylcholinesterase (HuAChE) and human serum butyrylcholinesterase (HuBuChE). The most promising biological activities have been shown by aromatic esters labelled as LC- 70 (IC50 HuAChE = 0,12 ± 0,01 µM) and LC-73 (IC50 HuAChE =0,17 ± 0,01 µM). The cytotoxic activity of prepared compounds has been...
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Preparation of lycorine derivatives and their biological activity
Lipovská, Kamila ; Cahlíková, Lucie (advisor) ; Kuneš, Jiří (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Botany Candidate: Kamila Lipovská Supervisor: doc. Ing. Lucie Cahlíková, Ph.D. Title of Diploma thesis: Preparation of lycorine derivatives and their biological activity The plants of the Amaryllidaceae family are one of the most important sources of biologically active alkaloids. Lycorine, a phenanthridine alkaloid, isolated from various species of the Amaryllidaceae plant family, has attracted considerable attention due to its promising biological activities. Specifically, its anticancer properties have been evaluated in vitro and in vivo in various preclinical models of human cancers. Further biological effects manifested by lycorine are: antiviral, antibacterial, antifungal, antiplasmodial, anti-oxidant, anti-inflammatory and insect antifeedant effects, as well as ascorbic acid biosynthesis and RNA inhibitory activity. So far, lycorine was used for preparation of many derivatives by modification of different functional groups in its molecule, and screened for a various biological activities such as anticancer activity, inhibition of cholinesterases, antiplasmodial, antitrypanosomal, antiviral and anti-Trichomonas vaginalis activity. The present work deals with the preparation of lycorine derivatives and their...
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Analysis of degree of the financial market regulation in the US and expected trends
Malyk, Kateryna ; Blahová, Naďa (advisor) ; Marková, Jana (referee)
The bachelor thesis is focused on the analysis of the US financial market regulation system and the investigation of certain cyclical events, which then lead to a change of regulation. The aim is to provide an overview of the real situation on the financial market. Another aim of this thesis is to highlight the existing significant issue in the US market and warn of possible consequences. Attention is also paid to the interconnection with the cycle of the US President's election. The first chapter generally describes the history of development and transformation of regulation in the United States. The second chapter focuses on the structure of the US financial market regulation and supervision system by regions. In the third part of the bachelor thesis, selected impulses of regulation change are analyzed and the current situation in the US market is described. The conclusion includes a summary and my opinion on the future development potential in the field of regulation.
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