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Evaluation of biological activity using Artemia salina
Kvapilová, Radka ; Vytlačilová, Jitka (advisor) ; Jahodář, Luděk (referee) ; Macáková, Kateřina (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Botany and Ecology Author: Mgr. Radka Kvapilová Supervisor: RNDr. Jitka Vytlačilová, Ph.D. Title of rigorous thesis: EVALUATION OF BIOLOGICAL ACTIVITY USING ARTEMIA SALINA Traditional Chinese medicine originated in ancient China and has evolved over thousands of years. TCM therapist use herbal medicines and body practices. Nowadays, Chinese medicine continues to develop and is used by millions of people around the world. The aim of this study was to evaluate the toxicity of these products - Epimedii herba, Salviae miltiorrhizae radix, Zanthoxyli fructus pericarpium, Nelumbinis folium a Gardeniae fructus. The experiment was conducted on organism Artemia salina. These experiments were evaluated after the 24 hours and the LC50 values were calculated. Toxicity declined in order: Zanthoxyli fructus pericarpium > Gardeniae fructus > Nelumbinis folium > Epimedii herba > Salviae miltiorrhizae radix. Key words: Zanthoxyli fructus pericarpium, Gardeniae fructus, Nelumbinis folium, Epimedii herba, Salviae miltiorrhizae radix, Artemia salina.
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Iron-chelating acitivity of selected alkaloids III.
Dočekalová, Linda ; Macáková, Kateřina (advisor) ; Siatka, Tomáš (referee)
Dočekalová L., Iron-chelating activity of selected alkaloids III, Diploma thesis, Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical botanic and ecology, Hradec Králové, 2016, 60 pp. Iron is important trace element necessary for human organism. When excess it develops free radicals and structures of organism are harmed. It can lead to organ failure. Excess is solved with chelators, the most used is deferoxamine. But his terapeutic regimen is disadvantageous and it has a lot of side effects. That's reason for searching for substances with better features. This paper focuses on studium of iron-chelating activity of selected alkaloids from family Amaryllidaceae. Concretely, it's galanthamine, undulatine, buphanisine, caranine, 1-O- acetylbulbisine, homolycorine, tazettine, galanthamine, chlidanthine, ambelline, haemanthamine, haemanthidine, hamayne, 9-O-demethylgalanthine and lycoramine. As standard for comparison of activity was used deferoxamine. Activity was measured by spectrophotometer. As indicator was used ferrozine. Chelatation was measured for ferrous ionts and for total iron, where hydroxylamine as reduction agent was used. Ferrous ionts was measured also with pH alteration. Highest activity reached deferoxamine in all executed measurements. In...
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Iron-chelating effects of flavonoid metabolites - small polyphenolic substances
Vavřichová, Nikol ; Macáková, Kateřina (advisor) ; Karlíčková, Jana (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical botanic and ekology Candidate: Nikol Vavřichová Supervisor: Ing. Kateřina Macáková Ph.D. Title of diploma thesis: Iron - chelating effects of flavonoid metabolites - small polyphenolic substances (2015/2016) Iron is a trace element which is necessary for function of an organism. There is no specific excretion mechanism for iron, therefore any deflection causes deficiency or abundance. Iron abundance leads to hemochromatosis. An application of iron chelators is a treatment of choice for hemochromatosis. There are three clinically used chelators for treatment of iron overload: deferoxamine, deferasirox and deferiprone. These drugs are inappropriate for therapy (side effects, dosage form). Therefore there is a place for serching for new types of medicine for treatment of hemochromatosis. Flavonoids are natural substances with positive influence on a human organism. The most investigated effects are antioxidant and chelating activity. As flavonoids are metabolised in a human body, there is an arising question if flavonoid metabolites are also able to chelate iron ions. For this work we chose derivates of benzoic acid: benzoic acid, 3 - hydroxybenzoic acid, 4 - hydroxybenzoic acid, 2,4 - dihydroxybenzoic...
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Natural products and their β-secretase inhibitory activity.
Kočová, Kateřina ; Chlebek, Jakub (advisor) ; Macáková, Kateřina (referee)
Kočová, K.: Natural compounds and their β-secretase inhibitory activity, Diploma thesis, Charles University in Prague, Faculty of Pharmacy in Hradci Králové, Department of Pharmaceutical Botany and Ecology, Hradec Králové 2015, 83 p. Data used in this Diploma Thesis have been taken from foreigner scientific literature. It provides the whole summary of natural compounds with β-secretase inhibitory activity. First chapter Alzheimer's disease briefly describes a definition, risk factors and symptomatology of the disease. Most of this chapter characterizes an etiopathology of the disease focused on amyloid theory. Finally there are also mentioned current approaches to therapy of Alzheimer's disease and those, which stay in clinical trials. Next part is dedicated to physiological functions and substrates of the β-secretase. This diploma thesis evaluates the current state of scientific research of synthetic inhibitors of β-secretase, describes the most important methods of testing inhibition and activity of β-secretase in vitro and outlines the issue of development of new inhibitors using in silico method. Main part of this work consists of the list of natural compounds with β- secretase inhibitory activity. This part is structured according to particular types of primary and secondary metabolites....
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Assessment of copper chelation of flavones by bathocuproine method
Michalicová, Alena ; Karlíčková, Jana (advisor) ; Macáková, Kateřina (referee)
Michalicová A., Assessment of copper chelation of flavones by bathocuproine method, Rigorous thesis 2013/2014, Charles University in Prague, Faculty of Pharmacy in Hradec Králové, pp.62. In the human body, copper is the third most widespread trace element. It is responsible for the proper function of various enzymes, which are involved in many important metabolic processes. The maintenance of copper homeostasis is essential for human and its disorders lead to different diseases and pathological changes. Plants produce a large number of metabolites, which are generally divided into primary and secondary. Secondary metabolism, built on primary metabolism, is not necessary for plant life, but offers a wide range of biological effects, used in medicine and pharmacy. Some secondary metabolites from the group of flavones also show chelating activity and are capable of forming chelating complexes with transition elements, such as copper, iron, etc. Thanks to their properties, they could introduce potential therapeutic solutions for copper homeostasis disorders. This thesis deals with the chelating activity of six flavones with the substitution on the ring A - 5-hydroxyflavone, baicalein, baicalin, chrysin, mosloflavone and negletein. Baicalein exhibited the highest chelating activity, while the baicalin...
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Alkaloids of family Amaryllidaceae: genus Lycoris.
Nekolná, Petra ; Cahlíková, Lucie (advisor) ; Macáková, Kateřina (referee)
Author: Petra Nekolná Title: Alkaloids of family Amaryllidaceae: genus Lycoris Diploma thesis Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany and Ecology 2015, 79 p. The aim of this diploma thesis was to summarize the findings about alkaloids which were isolated from Lycoris plants of Amaryllidaceae family. It contains a botanical characteristics of species of genus Lycoris which were studied phytochemically, a file of alkaloids which were isolated from these plants and findings about the biological activity of these compounds. Within the genus Lycoris 11 species were studied phytochemically and 118 alkaloids were isolated from these plants. Alkaloids which were isolated from Lycoris plants are divided in several structural groups. The lycorine-, homolycorine-, crinine-, galanthamine- and pancratistatine-type alkaloids occur the most numerously. Anticancer, acetylcholinesterase-inhibitory and antimalarial activity of the alkaloids were described. The biological activity of alkaloids is connected with their structure. The most significant anticancer activity was observed in alkaloids from lycorine-, crinine- and pancratistatine-type. Acetylcholinesterase-inhibitory activity was pronounced the most in galanthamine-type alkaloids. The most...
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Comparison of original Ellman's method and its modification using microplate reader
Morávková, Martina ; Macáková, Kateřina (advisor) ; Siatka, Tomáš (referee)
Morávková, Martina. Comparison of original Ellman's method and its modification using microplate reader. Diploma thesis 2015. Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany and Ecology. Supervisor: Ing. Kateřina Macáková, Ph.D. Key words: Ellman's method, acetylcholinesterase, butyrylcholinesterase, spectrophotometer, microplate reader. Ellman's method is often used procedure for measuring an inhibition of cholinesterases acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). The principle is based on hydrolysis of acetylthiocholiniodide and butyrylthiocholiniodide to give an appropriate acid and thiocholine. Amount of thiocholine is determined spectrophotometrically by reaction with 5,5'-dithiobis-2-nitrobenzoic acid. Results of measurement from two different devices (spectrophotometer and microplate reader) and at two different temperatures (room temperature and 37 řC) were compared in this thesis. Substances with different amount of inhibition of both enzymes were chosen: allocryptopine, californidine iodide, eserine, galanthamine, huperzine A and tazettine. For californidine iodide (AChE, BuChE), eserine (BuChE) and huperzine A (AChE) were detected statistically significant differences during measurement on different devices and at...
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Optimization of Oxidative Stress Diagnostic Methods
Mercová, Miroslava ; Macáková, Kateřina (advisor) ; Mladěnka, Přemysl (referee)
67 ABSTRACT Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Botany and Ecology Candidate: Mgr. Miroslava Mercová Consultant: Ing. Kateřina Macáková, PhD. Consultant - specialist: doc. RNDr. Miroslav Pohanka, PhD. Title of Thesis: Optimization of oxidative stress diagnostic methods Many methods have been developed to measure markers related to oxidative stress, but only little attention has been paid to their optimization for sample handling. Sample processing and storage can reduce stability of detected markers and therefore influence the results obtained. In this experiment we studied the effect of freezing - thawing cycles on the stability of some oxidative stress markers. The objective was to evaluate the process of repeated freezing as a potential risk factor that can interfere with the precision of measurements. Wistar rat tissue homogenates (brain, liver, heart, kidney, spleen) were frozen (-80 řC) and thawed at room temperature for five cycles. TBARS, FRAP, DPPH-test, GSH levels and GR activity were measured after the every freeze - thaw cycle. The measured data show changes in levels of the assessed markers. Their stability was affected in all of the tested samples, already after the first cycle. In many cases, we found strong linear dependence between...
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Iron-chelating acitivity of selected alkaloids I.
Rudolfová, Tereza ; Macáková, Kateřina (advisor) ; Karlíčková, Jana (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical botanic and ecology Candidate: Tereza Rudolfová Supervisor: Ing. Kateřina Macáková, Ph.D. Title of diploma thesis: Iron-chelating activity of selected alkaloids I. (2012-2013) Iron belongs among the essential trace elements in the human body, where takes many important functions. Metabolic disorder of iron occurs as iron deficiency (anemia) or its abundance (hematochromatosis). Production of free radicals is induced while the level of iron is increased. This has been observed in patients with Alzheimer's disease. Abundance of iron is treated by chelating agents (f.e. deferoxamine). Treatment takes place by slow infusion which is time-consuming and expensive. These are reasons of looking for new substances administrated orally. Alkaloids are products of secondary metabolism of plants. Big doses are toxic for body. Some of their properties can be used for treatment in low concentration. This work focuses on chelation activity of certain isoquinoline alkaloids (allocryptopine, berberine, bulbocapnine, eschscholtzine, galantine, lykorine, californidine, protopine, sinoacutine, sculerine and stylopine). Deferoxamine has been used as a standard. Chelation of Fe2+ ions and total iron, where hydroxylamine has...
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Biological Activity of Selected Taxons of Mushrooms from Divisions Ascomycota and Basidiomycota
Macáková, Kateřina ; Opletal, Lubomír (advisor) ; Kokoška, Ladislav (referee) ; Blunden, Gerald (referee)
Charles University in Prague, Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Botany and Ecology Candidate Ing. Kateřina Macáková Supervisor Doc. RNDr. Lubomír Opletal, CSc. Title of Doctoral Thesis Biological activity of selected taxons of mushrooms from divisions Ascomycota and Basidiomycota. Though they are relatively insufficiently explored, mushroom are considered to be important source of bioactive substances, which is evident especially in Asian countries where some species of mushrooms, eventually their extracts or substances isolated from them, are used for healing of some diseases. This study, which covers 357 tested species of mushrooms growing in Czech Republic, focuses especially on antioxidant activity of mushroom extracts (2,2'-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging and hydroxyl radical scavenging activity). Inhibitory activity towards human acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) was also observed. For determination of antiradical activity, DPPH radical scavenging assay with the use of sequential injection analysis and chemiluminescence method for hydroxyl radical scavenging with the use of luminol were utilized. Total amount of phenolic substances was determined in the most active species. The correlation analysis showed that...
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