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Antiprotozoal activity of natural compounds
Muchová, Michaela ; Vytlačilová, Jitka (advisor) ; Karlíčková, Jana (referee)
1 Abstract Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Botany and Ecology Author: Michaela Muchová Supervisor: RNDr. Jitka Vytlačilová, Ph.D. Title of diploma thesis: Antiprotozoal activity of natural compouds Increasing resistance to commonly used drugs in the treatment of protozoal infections has stimulated research of new drugs. Potential source of these new drugs could be found in natural substances. This thesis deals with testing of antiprotozoal activity of isoquinoline alkaloids berberine, palmatine and papaverine. The effect of individual tested compounds was observed on unicellular model organism Tetrahymena thermophila. Percentage inhibition of growth and reproduction of this protozoan was determined using 24-hour multi-generational test. Median inhibitory concentration 24hIC50 was calculated from the measured values. Papaverine showed the strongest antiprotozoal activity among testing compounds. Antiprotozoal activity decreased in the following order papaverine > palmatine > berberine. All alkaloids had stronger antiprotozoal activity than ornidazole, which was used as a standard antiprotozoal agent. Key words: antiprozoal activity, berberine, palmatine, papaverine, ornidazole, Tetrahymena thermophila
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Iron-chelating Properties of Selected Novel Chelators from 4-acyl-5-pyrazolone Group
Matula, Aleš ; Mladěnka, Přemysl (advisor) ; Karlíčková, Jana (referee)
4 ABSTRACT Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Pharmacology and Toxicology Candidate: Aleš Matula, MSc. Consultant: Dr. Přemysl Mladěnka, Ph.D. Title of Thesis: Iron-chelating properties of selected novel chelators from 4-acyl-5- pyrazolone group Both iron deficiency and iron overload play important roles in the pathophysiology of certain diseases. A suitable therapy in the case of iron overload represents the administration of iron chelators, especially in the treatment of hematological diseases, where the chronic iron overload occurs (a long-term usage of blood transfusions). The application of iron chelators for other diseases (acute myocardial infarction, cancer, etc.) appears as a promising tool as well. The current chelators suffer from a low level of compliance, efficiency, their poor activity in acidic environment or they reduce ferric ions to ferrous ions and that leads to oxidative stress. The subject of this thesis is to verify the iron-chelating properties of selected novel chelators from 4-acyl-5-pyrazolone group by use of UV-VIS spectrophotometric methods. Four compounds have been chosen: benzyl-, phenyl- and thienylderivatives of the basic structure and the derivative marked as H2Q4, which is a double molecule of the basic structure of...
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Ecotoxicological evaluation of the non-steroidal and anti-inflammatory drug
Horáková, Veronika ; Vytlačilová, Jitka (advisor) ; Karlíčková, Jana (referee)
Horáková Veronika, Ecotoxicological evaluation of the non-steroidal and anti- inflammatory drug, (graduation thesis) Charles University in Prague, Pharmaceutical Faculty in Hradec Králové, Department of Pharmaceutical Botany and Ecology; total number of pages: 67 There is getting more higher occurrence of residuals of healing substance connected with growing consumption of medicals in our environment, where they influence a range of organisms. In this work the ecotoxicity of diclofenac was monitored. Four tests of toxicity were selected for evaluation of this influence - one acute test (with Thamnocephalus platyurus), two semi-chronic tests (with Tetrahymena thermophila, Sinapis alba seeds) and one chronic test (with Brachionus calyciflorus). Values for diclofenac have been found from these tests: 24hEC50 5,058 mg/l - THAMNOTOXKIT FTM , 24h EC50 32,88 mg/l (23,07 - 46,86 mg/l) at 492 nm - more generation test with organism Tetrahymena thermophila, 48h EC50 1,363 mg/l (0,7848 - 2,366 mg/l) - ROTOXKIT F CHRONIC, 72h EC50 71,42 mg/l (62,51 - 81,60 mg/l) - a semi chronic test with Sinapis alba seeds. Key words: ecotoxicology, diclofenac, Tetrahymena thermophila, Thamnocephalus platyurus, Brachionus calyciflorus, Sinapis alba
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Alkaloids of plants from family Amaryllidaceae and their biological activiy (1960-2010)
Buková, Vladimíra ; Macáková, Kateřina (advisor) ; Karlíčková, Jana (referee)
Buková, V. Alkaloids of plants from family Amaryllidaceae and their biological activity (1960-2010). Charles University in Prague, Faculty of Pharmacy in Hradec Králové, 77 pp. The Amaryllidaceae family includes many species with important biological effects. This thesis is concerned with alkaloids of this family, their chemical structure, occurrence in particular species. Main goal of this thesis is to introduce their biological effects. The most important alkaloid of this family - galanthamin - acts as ecetylcholinesterase inhibitor and it is utilized for treating of the Alzheimer disease. The inhibitory effect on acetylcholinesterase has been described also at lycorin, 1-O-acetyllycorin, ungerenin, deoxylycorenin, montanin, hamayn and sanguinin. Amaryllidaceae alkaloids have also strong anticancer effects; an activity has been proved especially at alkaloids lycorin, pseudolycorin, pancratistatin, narciclasin, crinamin, heamanthamin, and others. From other important effects, it is necessary to mention antiprotosoal, antivirotic, antitrypanosomal, antibacterial, antiphlogistic, and antifungal activities.
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Study of inter-variant differences in xenobiotics metabolism in flax
Hartinger, Jan ; Skálová, Lenka (advisor) ; Karlíčková, Jana (referee)
Seed root inhibition tests with 18 species of flax (Linum usitatissimum) were carried out with different concentrations of TNT (trinitrotoluene) in order to elucidate intervarietous differences regarding their abilities to degrade nitrocompounds. The curves demonstrating dependency of root lengths on TNT concentrations varied significantly. The outcomes were influenced by the fact that five of the species germinated problematically even with the zero level of TNT. Callus cultures were grown from six of the species and cell suspension cultures were derived from three of them. Cell suspension cultures were tested on the ability to degrade TNT and DNT (dinitrotoluene) present in the medium. The decrease of TNT or, respectively, the decrease of DNT concentrations in the medium was measured by HPLC. It was discovered that contrary to TNT, DNT is very toxic for the cells when its concentrations get close to the level of maximum solubility. Trinitrobenzene, 2-aminodinitrotoluene and 4- aminodinitrotoluene were identified as main degradation products of TNT. Further on, 2D electrophoresis was performed with samples from cultures of two species stressed by DNT and TNT. In case of DNT an increase of protein density was marked in a certain area while in case of TNT no similarity was found between responses...
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Determination of artemisinin in Artemisia annua
Špundová, Jana ; Jahodář, Luděk (advisor) ; Karlíčková, Jana (referee)
This studies describes the determination of artemisinin in Artemisia annua L. cultivated in Czech Republic in 2006. Plant was harvested in four vegetative stages (intensive vegetative growth stage, bud formation, cease bloom stage and maturity seed stage). Plant was shade dried on the air and extracted with an organic solvent hexane for 17 hours and then filtrated. Artemisinin was confirmed by thin layer chromatography with artemisinin standard use. The concentration of artemisinin was determinated by reversed phase high performance liquid chromatography with constant constitution of mobil phase and UV detection with wave length 295 nm. Maximum artemisinin concentration occured at the bud formation stage (0,030%).
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Biological activity of plant metabolites IX. Antimicrobial activity of some secondary metabolites
Váňová, Jana ; Opletal, Lubomír (advisor) ; Karlíčková, Jana (referee)
Váňová, J.: Biological Activity of Plant Metabolites IX. Antimicrobial Activity of Some Secondary Metabolites. Diploma Thesis, Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany and Ecology, Hradec Králové 2008, 62 pp. The antibacterial activity of 4 selected plant extracts was evaluated against E. coli O157:H7 and Staphylococcus aureus. Extracts were prepared by extraction in 80% ethanol and subsequent percolation. Two methods were used for determination of minimal inhibitory concentration (MIC). In the first case they were not reached the values of MIC expected for E .coli on the basis of the other literature studies. All samples within the concentration range of 5 - 0,005 ppm which were prepared in two series were negative even after 48 hours exposition. In the second case it was reached better results for E. coli and S. aureus. Two series of serial twofold dilutions within the concentration range of 25 %-0.02 % were prepared. The lowest values of MIC were exhibited by Thymus vulgaris extract, especially against Gram-positive indicator strain. Nevertheless the values of MIC remain very high (3.13 % for E. coli, 0.2 % for S. aureus). For determination of minimal bactericidal concentration (MBC) in E. coli O157:H7 and E. coli O55 seven...
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Phytochemical study of Helianthus annuus L. IV
Podlipná, Jana ; Karlíčková, Jana (advisor) ; Opletal, Lubomír (referee)
Podlipná, J. Phytochemical study of Helianthus annuus L. IV. Diploma thesis 2008. Charles University in Prague, Faculty of Pharmacy in Hradec Králové, 93 pp. The thesis was focused on phytochemical research of plant Helianthus annuus L. The aim of the research was to obtain new information about plant metabolites of sunflower. There was an effort to evaluate the quality of included compounds in sprouts and sunflower seed shells and to divide ethanolic extract from leaves of this plant. Finally the evaluation of biological activity was done from fractions of leaves and shells. There weren't detected any alkaloids in extract from sprouts. Caffeic acid was detected in sunflower seed shells according to thin-layer chromatography. 80% ethanolic extract from sunflower leaves had significant antioxidant activity which was measured both by DPPH radical and FRAP method. Fat acids were found in fraction No. 14 (from 2nd chromatographic column of extract from leaves). Extract from leaves was toxic for worms Tubifex tubifex Müll. but it wasn't phototoxic.
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Influence of enzymatic activity induced by copper and cadmium in aquatic plant Myriophyllum alterniflorum DC.
Mikšová, Martina ; Karlíčková, Jana (advisor) ; Macáková, Kateřina (referee)
This thesis concerns with the effects of heavy metals on plants and is a part of a broader research on biomarkers of oxidative stress in aquatic plants in the Department of Pharmaceutical Botany of Faculty of Pharmacy in the University of Limoges. Experimental organism was an aquatic plant Myriophyllum alterniflorum DC (alternate water milfoil) that was collected in the upper stream of the river Vienna. Samples were cultivated in the increasing concentrations of copper and cadmium (0mM, 0,25mM, 0,5mM, 0,75mM) for 1, 3 and 6 days. On account of time and chemical products insufficiency only several analyses of plants treated with copper were carried out. Catalase is one of the enzymes integrated in the antioxidative defence system. It decomposes H2O2 into water. During the time catalase activity gradually increased up to 0,5mM. 0,75mM showed the maximum after the third day. When comparing different copper concentrations after the same cultivation period the highest activity was observed in 0,25mM in the first day and in 0,50mM the third and sixth day. Myriophyllum alterniflorum DC as other aquatic plants exhibits the heavy metal accumulation ability increasing in time and higher copper concentrations. On the contrary, decreasing time and concentration dependence was observable in measurements of...
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