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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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Analysis of Andrographis leaves extract
Tonarová, Marta ; Jahodář, Luděk (advisor) ; Macáková, Kateřina (referee)
1 CHARLES UNIVERSITY IN PRAGUE FACULTY OF PHARMACY IN HRADEC KRÁLOVÉ DEPARTMENT OF PHARMACEUTICAL BOTANY AND ECOLOGY Analysis of Andrographis leaves extract. Marta Tonarová, 2010 Abstract: The analysis of the extract of leaves Andrographis paniculata (Acanthaceae) was accomplished. The commercial ethanol extract with the contents of andrographolides not higher than 10 % represented the tested material. In case of using the standard andrographolide, the thin layer chromatography has proved its very low amount in the extract only, in spite of the fact that studying literature consideres its contents as majority. The identity of the standard was verified by mesuring its NMR spectrums, which refers to the informations in the studying literature. Contents of andrographolides was fixed by the high performance liquid chromatography extanded to the standard, with using of isocratic elution and spectrophotometric detection by the wave lenght 223 nm. Total contents of the andrographolides in the extract was 12,23 % and consequently it refers to the production protocol. The main component in the contents of the extract was isolated by using preparative TLC. On the basis of fixing the NMR spectrums and their confrontation with the studying literature it was determined as 14-deoxy-11,12-didehydroandrographolide.
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Toxicity of thiosalicylanilides with invertebrate organisms
Čapková, Zuzana ; Vytlačilová, Jitka (advisor) ; Macáková, Kateřina (referee)
Thiosalicylanilides are important biologically active substances. They have been used for they anthelmintic and antifungal activity for a long time. In recent years they were tested as substances potentially effective in the therapy of tuberculosis. This Diploma-Study presents the toxicity of newly synthesized thiosalicylanilides. As these substances are hardly soluble or practically insoluble in water, dimethylsulfoxide was succesful as a co-solvent in the experiments. The Artemia franciscana biotest was used as a screening method. These experiments were evaluated after a 24hours period and the EC50 values were calculated. This method is rapid, inexpensive and convenient for pre-screening toxicity tests. The toxicity order for the tested compounds was: 4' - bromo - 3,5 - dichlorothiosalicylanilide (13e) > 3,4',5 - trichlorothiosalicylanilide (13b) > 3', 4'- dichlorothiosalicylanilide (8c) > thiosalicylanilide (8a) > 5 - chlorothiosalicylanilide (12a) > 4'- methylthiosalicylanilide (8i).
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Biological activity of macromycetes - D
Pásztó, Lenka ; Macáková, Kateřina (advisor) ; Siatka, Tomáš (referee)
Charles University in Prague, Faculty of Pharmacy in Hradec Králové Department Department of Pharmaceutical Botany and Ecology Candidate Mgr. Lenka Pásztó Consultant Ing. Kateřina Macáková Ph.D. Title of Thesis Biological activity of macromycetes - D Keywords: fungi, cholinesterase inhibition activity, phenolic compounds, alkaloids, Alzheimer disease, antioxidant activity. In this thesis, altogether 15 fungal species from the families Bolbitaceae, Cortinariaceae a Tricholomataceae were tested for their biological activities. The extracts of all species were assessed for the alkaloid content with the use of thin- layer chromatography (TLC). Significant content of alkaloid substances was not detected in any of the tested mushroom species. All fungal extracts were also tested for their cholinesterases inhibition activity using Ellman's spectrophotometric method with 5,5'-dithiobis-2-nitrobenzoic acid. The highest inhibition activity against erythrocyte AChE was indicated in the case of Mycena galericulata extract, and against serum BuChE in the case of Gymnopilus sapineus. Nevertheless, in comparison with values of standard inhibitors (galanthamine and huperzine A), the inhibition activity of both extracts was negligible. Finally, Folin-Ciocalteu's method was applied to set an amount of phenolic...
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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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Evaluation of antiprotozoal activity by Tetrahymena pyriformis
Osecká, Daniela ; Vytlačilová, Jitka (advisor) ; Macáková, Kateřina (referee)
74 ABSTRACT Title of thesis Evaluation of antiprotozoal activity by Tetrahymena pyriformis Charles University in Prague Faculty of Pharmacy in Hradec Kralove Department of Pharmaceutical Botany and Ecology Candidate: Daniela Osecká Consultant: Mgr. Jitka Vytlačilová The protozoal pathogens are causing asymptomatic and symptomatic infections. The risk of the disease threatens to almost every man, therefore it is very important the antiprotozoal therapy. Tetrahymena pyriformis is a unicellular organism, which we tested out under the action of three substances, albendazole, mebendazole and ornidazole. We used two methods applied to measuring the viability of protozoan. It is a basic method for testing the inhibition of growth of the organism Protoxkit FTM using the conversion of food biomass in suspension of infusorian and MTT method, which uses the reduction of MTT dye (3 - [4,5-dimethyl-thiazol-2-yl] -2,5-diphenyl-tetrazolium bromide). Spectrophotometrically from the measured data, we build tables and charts, optical density, depending on the time of culture and calculated percent inhibition for five descending concentrations of test substance. Our aim was to determine whether all the test substances showing the antiprotozoal activity. The greatest toxicity showed albendazole (method Protoxkit FTM at the...
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Screening of alkaloidal plants for antioxidant and anticholinesterase activity in vitro II.
Pšeničková, Jana ; Macáková, Kateřina (advisor) ; Karlíčková, Jana (referee)
Pšeničková, Jana. Screening of alkaloidal plants for antioxidant and anticholinesterase activity in vitro II. Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany and Ecology. 57 pp. Supervisor: Ing. Kateřina Macáková, Ph.D. Keywords: cholinesterase inhibition activity, antioxidant activity, alkaloids, Alzheimer's disease, oxidative stress Selected plant species of the families Papaveraceae, Fumariaceae and Ranunculaceae were tested in terms of this thesis. Alkaloid content was evaluated by a thin-layer chromatography (TLC); ethanol and alkaloid extracts were tested for their cholinesterase inhibitory activity and antioxidant activity. All of the studied species were tested for the cholinesterase inhibition activity by the Ellman's spectrophotometric method using the 5,5'-dithiobis-2-nitrobenzoic acid. The activity of extracts was compared with IC50 values of common inhibitors of cholinesterases: galanthamine (IC50 HuAChE = 2.59 ± 0.065 μg/ml, HuBuChE = 58.02 ± 1,30 μg/ml), and huperzine A (IC50 HuAChE = 0.061 ± 0.001 μg/ml, HuBuChE 1000 μg/ml). The highest cholinesterase inhibitory activity from the tested specimen showed ethanol extract from the aerial part of Glaucium corniculatum (IC50 AChE = 0,39 µg/ml, IC50 BuChE = 4,27 µg/ml). The species...
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Analysis of compounds contained in Acer platanoides L. flowers
Rajdlová, Stanislava ; Karlíčková, Jana (advisor) ; Macáková, Kateřina (referee)
SUMARY Extraction of compounds from flowers Acer platanoides was carried out in the first part of our work. Two extracts have been prepared - ether and ethanol. Identification of the compounds was done by the help of a thin layer chromatography with using the standards of phenolic compounds. According to the results TLC the presence of rutin, apigenin, hesperetine, hyperoside and chlorogenic acid were supposed. The presence of a compound of reducing character was proved in the ether extract. The HPLC analysis confirmed the presence of rutin in the ethanol extract. Further, the content of total phenolic compounds was determinated in the ethanol extract and results were expressed as gallic acid equivalent, i.e. 0,135 mg GAE/mg of extract. The second part of our work was aimed at testing antioxidant activity of ethanol extract by help of DPPH test. Very high values of antioxidant activity have been measured. Compounds of phenolic character were supposed to participate in antioxidant activity of ethanol extract.
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Analytical methods of evaluation of antioxidant/free-radical scavenging activity
Baronová, Pavlína ; Macáková, Kateřina (advisor) ; Karlíčková, Jana (referee)
Baronová, P. Analytical methods of evaluation of antioxidant/free-radical scavenging activity. Charles University in Prague, Faculty of Pharmacy in Hradec Králové, 65 pp. Antioxidant active compounds play a positive role in the prevention and threatment of many diseases. Consequently, antioxidant activity of natural and synthetic compounds is world-widely investigated. For this purpose, many methods for the evaluation of the activity were elaborated. The first part of this review is focused on the describtion of free radicals, its origin and function in the human body. Antioxidants are divided into several subclasses like endogenous and exogenous, which are divided to high-molecular or low molecular according to the structure, and synthetic and natural according to the origin. The methods for determination of free radicals (synthetic or endougenous radicals) scavenging activity, evaluation of inhibition of lipid peroxidation, or redox properties (chemical or elektrochemical methods) of tested compounds are enclosed in this thesis. The instrumetnal analytical methods like HPLC or SIA (sequential injection methods) and FIA are also mentioned. The review also describes the practical examples of use of various described methods. In the conclusion, the advantages and disadvantages of individual methods...
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Biologically active metabolites of plants. 4. Alkaloids from Eschscholtzia californica CHAM. and their biological activity.
Bednaříková, Lucia ; Cahlíková, Lucie (advisor) ; Macáková, Kateřina (referee)
Bednaříková L.: Biologically active metabolites of plants 4. Alkaloids from Eschscholtzia californica CHAM. and their biological activity. Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany and Ecology, Hradec Králové, 2011. Diploma thesis. 65 p. The aim of the diploma thesis was to process the pool of quaternary alkaloids from Eschscholtzia californica CHAM. (Papaveraceae). By means of column chromatography two alkaloids were isolated and subsequently subjected to structural analysis (MS and NMR studies). The first substance was identified as a tertiary alkaloid allocryptopine, the second one was a quaternary base californidine. Both alkaloids have previously been isolated from E. californica. Both substances were tested for their inhibitory activity against human erythrocyte acetylcholinesterase (HuAChE) and human plasma butyrylcholinesterase (HuBuChE). The measured values for allocryptopine were IC50 (HuAChE) = 250 ± 22,2 μM and IC50 (HuBuChE) = 530 ± 28,2 μM. Californidine's values were IC50 (HuAChE) = 36,7 ± 0,9 μM and IC50 (HuBuChE) >1000 μM. Galanthamine (IC50 (HuAChE) = 6,9 ± 0,3 μM, IC50 (HuBuChE) = 156 ± 6,9 μM) and huperzine A (IC50 (HuAChE) = 0,25 ± 0,01 μM, IC50 (HuBuChE) >1000 μM) were used as positive controls. In comparison to...
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