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Osecká, Karolína. "Možnosti ovlivnění vstřebávání kofeinu z kolových nápojů." Master's thesis, Vysoké učení technické v Brně. Fakulta chemická, 2014. http://www.nusl.cz/ntk/nusl-217018.
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This diploma thesis was focused on basic physicochemical properties of caffeine and investigation of the interaction between the polysaccharide sodium hyaluronan (HA), pectin (PEC) or lignohumate (HUM) and the alkaloid caffeine (CAF). The reason why this thesis was focused on study of aqueous solutions of hyaluronan or pectin with caffeine is that the presence of polysaccharide- caffeine complex could be beneficial for slowing the absorption of caffeine. In the theoretical part of the diploma thesis there is described a group of alkaloids, which caffeine belongs to and also polysaccharides hyaluronic acid and pectin. The most attention has been paid to caffeine, its properties and effects on the human organism. This diploma thesis also deals with non-alcoholic beverages with caffeine, 4-methylimidazole, and phosphoric acid. The last chapter of the theoretical part is dedicated to fluorescence spectroscopy. In the experimental part of this work I deal with the basic properties of caffeine and interaction between the caffeine and selected polysaccharides or lignohumate. At first, the chemical and physical properties of caffeine were determined. Based on these results the interaction of caffeine and hyaluronan or pectin was studied by using the fluorescence and absorbance. The HA of molecular weight of 1,7 MDa and pectin from citrus fruits were chosen for the study of the interaction with the caffeine. These two substances were mixed with the caffeine of concentration contained in Coca-Cola. The results of interaction that would lead to the influence of the emission or absorption properties of caffeine, were not proved. As a part of the work there was determined how pectin behaves in strongly acidic solution and then there was monitored the pH, conductivity and solubility of caffeine in water by using thermogravimetry and visual experiments. The obtained results of the interaction of hyaluronan-caffeine, pectin caffeine or caffeine-lignohumate can be used for description of the behavior of caffeine in the presence of selected polysaccharides and natural organic substance.
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Pipková, Renata. "Měření celkových alkaloidů v tabáku." Master's thesis, Vysoké učení technické v Brně. Fakulta chemická, 2011. http://www.nusl.cz/ntk/nusl-216798.
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The aim of this diploma thesis is the assay of total alkaloids in different tobacco types. To measure the content of total alkaloids are utilized types of tobacco used for preparation of tobacco blends and consecutive production of cigarettes. The samples of analyzed tobacco include various countries of cultivation and different crop years. There is described tobacco as a plant, in it contained alkaloids and the utilization of tobacco in the theoretical part. In more detail it deals with the production and construction of cigarettes which is closely related to the content monitoring of total alkaloids in tobacco. The contents of total alkaloids are determined by the continuous flow analyzer- SKALAR. On this spectrophotometer are set the contens of reducing sugars as well. The comparison of total alkaloids contents and reducing sugars from the perspective of single tobacco types, countries of cultivation and crop years is clearly summarized in the experimental part of the thesis that was performed in the company Philip Morris ČR, a.s.
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Panenková, Kristýna. "In vitro anti-proliferační aktivita alkaloidů čeledi Amaryllidaceae." Master's thesis, Česká zemědělská univerzita v Praze, 2016. http://www.nusl.cz/ntk/nusl-257583.
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Summary
Natural phytochemicals are currently used in the treatment of many diseases. Cancers are just ones of them and they are ranked among the most common and the most serious. Phytochemicals in the form of cytostatics are used in chemotherapeutic treatment of cancer. In future there could be included among cytostatics also some alkaloids from the family
of Amaryllidaceae, whose testing for a selective cytostatic effect on tumor cell lines
of colorectal carcinoma Caco-2 and HT-29 and on normal cell lines of human intestinal epithelial FHs 74 Int is a subject of this thesis.
There were tested 17 alkaloids isolated from plants of Chlidanthusfragrans, Zephyranthes robusta and Nerine bowdenii. Particularly alkaloids from plant Zephyranthes robusta namely haemanthamine with this values: IC50 = 0.99 plus/minus 0.14 microM for tumor cells, Caco-2, 0.59 plus/minus 0.01 microM for tumor cells HT-29 and 19.47 plus/minus 8.86 microM for normal cells
FHs 74 Int, Lycorine with values IC50 = 0.99 plus/minus 0.08 microM for tumor cells Caco-2, 1.2 plus/minus 0.01 microM for tumor cells HT-29 and 22.68 plus/minus 0.09 microM for normal cells FHs 74 Int and Haemanthidin with values IC50 = 3.29 plus/minus 0.91 microM to tumor cells Caco-2, 1.72 plus/minus 0.11 microM to tumor cells HT-29, and 11.63 plus/minus 0.86 microM for normal cells FHs 74 Int proved a significant
anti-proliferative activity.
From these results there is evident the selectivity against colorectal cancer cell lines. For this reason, those tested alkaloids are suitable for further testing and for study of their biological activity against tumor cells in the terms of in vitro and in vivo.
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Hroncová, Zuzana. "Mikrobiota trávicího traktu včel a příbuzného hmyzu a faktory ovlivňující její složení." Doctoral thesis, Česká zemědělská univerzita v Praze, 2016. http://www.nusl.cz/ntk/nusl-261408.
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This thesis consists of six research chapters, out of which, five have already been published in research journals, 1 is in the process of submission and the last chapter presents original unpublished confidential data in the process of manuscript preparation.
The research presented in this thesis concerns the complex mechanisms of bees and wasps immune system focused on microbiota as component of immunity. As shown in the introduction, highly social and managed species of bees like honey bees and bumble bees, play key roles in natural and agricultural ecosystems worldwide. Recent losses of bees have been attributed to pesticide exposure, poor nutrition, increased parasite loads and habitat degradation. Over the past several years, governments, beekeepers, and the general public worldwide have become concerned by increased losses of honey bee colonies, calling for more research on how to keep colonies healthy. Our main aim was to explore the complex mechanisms of bees and related species gut bacterial populations, their links to insect immunity and investigate the opportunities for an intervention. Part of our aim was to characterise the bumble bee and wasp gut microbiota using 16S RNA sequencing in a search for potentially novel bacterial species.
We have tried to explain how microbiome interacts with the host and showed that major members of these communities appear to benefit the host. The simple gut communities of social bees present ideal model systems to investigate the underlying evolutionary and genetic processes of such interactions. Information based on our results may help in the design of proper probiotic supplementation strategies with respect to physiological conditions in the honey bee gut.
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Witt, Anette. "Synthetic development towards benzodiazepine alkaloids : total synthesis of circumdatin F and C /." Stockholm, 2002. http://diss.kib.ki.se/2002/91-7349-077-6/.
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Jánská, Lucie. "Alkaloidy čeledi Amaryllidaceae: rod Zephyranthes." Master's thesis, 2018. http://www.nusl.cz/ntk/nusl-382766.
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Author: Lucie Jánská Název: Alkaloids of family Amaryllidaceae: genus Zephyranthes Diploma thesis Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of Pharmacognosy 2018, 75 p. The aim of this diploma thesis was to summarize all knowledge about alkaloids izolated from Zephyranthes plants of Amaryllidaceae family. It contains a detail overview of botanical charactericts of phytochemically studied plants of the genus Zephyranthes. Also the overview of alkaloids with bilogical activity was described. Within the genus Zephyranthes 10 species were studied phytochemically and 89 alkaloids were isolated from this plants. This alkaloids are divided in several structural groups. The lycorine-, haemanthamine-, galanthamine- and pancratistatine-type alkaloids occure the most frequently. Acetylcholinesterase-inhibitory, anticancer and antimalarial activity of the alkaloids was described like the most important. The most significant acetylcholinesterase- inhibitory activity was observed in alkaloids from galanthamine sctructural type. Anticancer activity was found the most in lycorine-, pancratistatine- and haemanthamine- type alkaloids. The most notable antimalarial activity was observed in lycorine- and heamanthamine- type alkaloids. Keywords Zephyranthes, Amaryllidaceae,...
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Öhlschlegelová, Jana. "Alkaloidy čeledi Amaryllidaceae: rod Hippeastrum." Master's thesis, 2019. http://www.nusl.cz/ntk/nusl-403945.
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Author: Jana Öhlschlegelová Title: Alkaloids of family Amaryllidaceae: genus Hippeastrum Diploma thesis Charles University, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany 2019, 74 p. Keywords: Hippeastrum, Amaryllidaceae, alkaloids, antiproliferative activity, Alzheimer's disease, cholinesterase inhibitors, galanthamine The aim of this diploma thesis was to unify current findings about alkaloids isolated from selected plants of the Hippeastrum genus in the Amaryllidaceae family. The fytochemical characteristics of the examined species was introduced, and a group of alkaloids which were isolated from these plant species was composed. Also, the biological activity was evaluated. Up to date, at least 13 plant species of the Hippeastrum genus were examined from the fytochemical perspective. Out of these species examined, 56 different alkaloids with defined structure were isolated. The isolated alkaloids are divided into several groups based on their structure. Namely, these are lycorine, homolycorine, crinine, galanthamine, narciclasine, tazettine, haemanthamine and montanine structural types. Also, alkaloids which differed structurally from these basic types were found in several plants studied. In the substances gained, the antiproliferative activity, inhibitory activity...
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Hodulová, Adéla. "Alkaloidy čeledi Amaryllidacee: rod Nerine." Master's thesis, 2018. http://www.nusl.cz/ntk/nusl-389079.
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Author: Adéla Hodulová Title: Alkaloids of Amaryllidaceae family, genus Nerine Diploma thesis Charles University, Faculty of pharmacy in Hradec Králové, Department of Pharmaceutical botany 2018, 51 p. The aim of this diploma thesis was to summarize up the findings about alkaloids which where isolated from genus Nerine plants of Amaryllidaceae family. There was introduced a botanical characteristic of the phytochemical studied species of the genus Nerine. The most studied species was Nerine bowdenii. All the knowledges about mentioned alkaloids were sum up. Ten species have been phytochemical studied out of the genus Nerine until now. In total, 40 alkaloids were isolated from these plants. Alkaloids which where isolated from the Nerine are divided into several structural types. Anticancer, acetylcholinesterase-inhibitory of the alkaloids were described. The biological activity is connected with their stucture. The most significant anticancer activity was observed in alkaloids from crinine- and lycorine type . Acetylcholinesterase-inhibitory activity was pronounced the most in crinine-type alkaloids. Keywords: Nerine, Nerine bowdenii, Amaryllidaceae, alkaloids
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Nekolná, Petra. "Alkaloidy čeledi Amaryllidaceae: rod Lycoris." Master's thesis, 2015. http://www.nusl.cz/ntk/nusl-335193.
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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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Kiełczewska, Urszula. "Synteza analogów alkaloidów steroidowych." Phd thesis, 2020. http://hdl.handle.net/11320/10193.
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Alkaloidy Solanum zostały wyizolowane z roślin pochodzących z rodziny psiankowate (Solanaceae), rodzaju psianka (Solanum). Są to alkaloidy steroidowe, których budowa opiera się na szkielecie cholestanu. Głównymi przedstawicielami tej klasy związków są solasodyna, tomatydyna oraz solanidyna. Alkaloidy steroidowe mają różnorodne właściwości biologiczne m.in.: antyproliferacyjne, neurogenne, przeciwdrgawkowe i przeciwzapalne. Szerokie spektrum aktywności biochemicznych i niskie stężenie w materiale roślinnym tych związków, zainspirowały chemików do projektowania ich syntetycznych analogów. Znanym przedstawicielem grupy alkaloidów Solanum jest solasodyna, będąca azotowym analogiem diosgeniny. Wydaje się, że to właśnie ten związek jest dobrym substratem w syntezie solasodyny i jej pochodnych. Proponowane dotychczas syntezy solasodyny z diosgeniny oparte są na trzystopniowej strategii: otwarcie pierścienia F (etap I), podstawienie grupy opuszczającej łańcucha bocznego nukleofilem azotowym (etap II) i zamknięcie pierścienia F (etap III). Prowadzone przeze mnie badania koncentrowały się na projektowaniu nowych analogów alkaloidów steroidowych, syntezie solasodyny i jej analogów oraz na ocenie ich aktywności biologicznej. Jednym z założeń niniejszej dysertacji było opracowanie dogodnej strategii jednoczesnego otwarcia pierścienia F w diosgeninie i wprowadzenie atomu azotu w strukturę steroidu (wykorzystanie azydków bądź karbaminianów). Utworzona w ten sposób 26-azotowa pochodna diosgeniny mogłaby posłużyć jako intermediat w syntezie solasodyny i jej analogów. Prowadzone w tym kierunku badania zaowocowały skróceniem znanych i opisanych w literaturze metod otrzymywania solasodyny i opracowaniem dwuetapowej syntezy piwalanu solasodyny z piwalanu diosgeniny. Podjęłam również bezpośrednie próby przekształcenia układu spiroketalowego (diosgenina) w spirosolanowy (solasodyna) za pomocą nowego odczynnika – amidku diizobutyloglinowego, który można łatwo otrzymać z wodorku diizobutyloglinu (DIBAL) i chlorku amonu. Prowadziłam również badania w kierunku znalezienia metody syntezy 26a-F-homo-, 22a(N)-F-homo analogów solasodyny i ich N-podstawionych pochodnych. Założyłam bowiem, że związki z 7-członowym pierścieniem F mogą wykazywać podobne właściwości biologiczne jak ich macierzyste substraty. Zsyntezowane pochodne zostały przebadane pod kątem właściwości antyproliferacyjnych i przeciw-neurodegeneracyjnych. W swojej pracy poszukiwałam również metod syntezy innych aza-steroidów. Były nimi pochodne pirymido-benzimidazolu, które uzyskałam w wyniku reakcji kondensacji octanu 16-dehydro-pregnenolonu z 2-aminobenzimidazolem. Optymalizacja warunków reakcji (wpływ katalizatora, czasu reakcji, rozpuszczalnika, stężenia poszczególnych reagentów), pozwoliły otrzymać łącznie 6 nowych analogów. Uzyskane pochodne wykazały bardzo dobrą aktywność przeciwnowotworową względem linii komórkowych raka prostaty. Wyniki eksperymentów przeprowadzonych w ramach niniejszej dysertacji zostały opisane w 5 publikacjach o zasięgu międzynarodowym oraz były prezentowane na licznych konferencjach zagranicznych i krajowych.Solanum alkaloids were isolated from plants of the family Solanaceae (Solanum). These are steroidal alkaloids whose structure is based on the C27 cholestan skeleton. The main representatives of this class of compounds are solasodine, tomatidine and solanidine. Steroidal alkaloids are known to possess a variety of biological properties such as: antiproliferative, neurogenic, anticonvulsant and antiinflammatory. The wide range of biochemical activity and the low concentration of these compounds in plant material inspired chemists to design their synthetic analogues. The most famous representative of this group of compounds is solasodine – a nitrogen analog of diosgenin. Thus it seems to be the first-choice starting material for the synthesis of solasodine derivatives. The solasodine syntheses from diosgenin proposed so far are based on three-stage strategy: F-ring opening (stage I), nitrogen nucleophile substitution of the side chain leaving group (stage II) and F-ring closure (stage III). My research was focused on designing, synthesis and evaluation of biological activity of solasodine and analogues. The main purpose of this dissertation was to develop a convenient strategy for the simultaneous opening of the F ring and the nitrogen atom introduction in the C26 position (with the use of eg. azides, carbamates) which may constitute promising method for obtaining the solasodine and its derivatives. The research carried out in this strategy allowed for the development of a two -step synthesis of solasodine pivalate. I also studied an attempt of a direct transformation of spirostanes (diosgenin) into spirosolanes (solasodine) by a new reagent – diisobutylaluminum amide, readily available from diisobutylaluminum hydride (DIBAL) and ammonium chloride. I was looking for the paths of the syntheses of 26a-homo-, and 22a(N)-homo analogues of solasodine and their N-acyl derivatives. I assumed that the derivatives with 7-membered F ring might exhibit similar biological properties to their parent compounds. The synthesized derivatives were tested for their antiproliferative and antineurodegenerative properties. In my research, I was looking for methods of synthesis other aza-steroids, including pyrimidobenzimidazole derivatives which were obtained by condensation of 16-dehydropregnenolone acetate with 2-aminobenzimidazole. The optimized reaction conditions (influence of the catalyst, reaction time, type of solvent, concentration of individual reactants) allowed to obtain a total of 6 new analogues. The obtained derivatives showed very good antitumor activity against prostate cancer cell lines. All obtained results of my presented in this dissertation have been described in 5 international publicat ions and have been presented at numerous foreign and national conferences.
Uniwersytet w Białymstoku. Wydział Chemii.
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Gábrlová, Lucie. "Alkaloidy čeledi Amaryllidaceae a jejich biologická aktivita." Master's thesis, 2016. http://www.nusl.cz/ntk/nusl-345647.
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Charles University in Prague, Faculty of Pharmacy in Hradci Králové Department of Pharmaceutical Botany and Ecology Lucie Gábrlová Diploma thesis: Alkaloids of family Amaryllidaceae and their biological activity The aim of this diploma thesis was to compile assigned fraction of alkaloidal extract obtained from Chlidanthus fragrans and isolation of at least two alkaloids for testing their biological aktivity. For the processing of the extract and isolation of the alkaloids contained in it was used preparative TLC. The obtained substances were then undegone structure analysis, specifically, there were used EI-MS and NMR methods. Based on the results obtained were isolated substances identified and prepared for screening of their biological activity, which was not part of this diploma thesis anymore. The isolated alkaloids were identified as 6α-hydroxybuphanidrine, crinamidine and crinine. 6α-Hydroxybuphanidrine failed to get enough for biological testing. Inhibitory activity of crinamidine and crinine against erythrocyte AChE and serum BuChE was quite weak. Equally, neither of alkaloids showed stronger ability to inhibit the POP, where for crinamidine was determined IC50 = 0,790 ± 0,062 mM and for crinine IC50 = 1,473 ± 0,122 mM. The measurment of cytotoxic activity has been carried out only with...
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Klátilová, Anežka. "Alkaloidy Vinca minor (Apocynaceae) a jejich biologická aktivita." Master's thesis, 2018. http://www.nusl.cz/ntk/nusl-388890.
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Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical botany Candidate: Anežka Klátilová Supervisor: doc. Ing. Lucie Cahlíková Ph. D. Title of diploma thesis: Alcaloids of Vinca minor (Apocynaceae) and their biological activities The aim of this diploma thesis was to process the assigned fraction isolated from the Vinca minor L. plant and to isolate at least one alkaloid to test its biological activity. Using preparative TLC, the alkaloid was sequentially isolated from the fraction, which was then subjected to a structural analysis. NMR and EI-MS methods were used herein. Thanks to these analyzes, the alkaloid was identified as venoterpine. Furthermore, the alkaloid was prepared to test for biological activity. Thus, the isolated alkaloid was identified as venoterpine and tested for biological activity. The observed inhibitory concentration (IC50) to HuAChE and HuBuChe was more than 500 μM, indicating that venoterpine does not rank as a significant inhibitor of cholinesterase. Likewise, the value of cytotoxic activity, when this activity was found to be greater than 10 μM to colorectal cancer cells as well as to healthy cells, is not significant. Key words: Vinca minor, Apocynaceae, alkaloids, biological activities
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ROZSYPALOVÁ, Adéla. "Chemická obrana slunéček proti mravencům." Master's thesis, 2009. http://www.nusl.cz/ntk/nusl-50361.
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This work studied distastefulness of alkaloids of eight ladybird species (Adalia bipunctata, Calvia quatuordecimguttata, Coccinella septempunctata, Cynegetis impunctata, Exochomus quadripustulatus, Halyzia sedecimguttata, Harmonia axyridis, Psyllobora vigintiduopunctata) for ants Lasius niger. The reaction to extracts of various ladybird species isn´t corelated with their size. There is a weak relationship of distastefulness on ladybird coloration.
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Bystrońová, Beáta. "Hodnocení alkaloidů pomocí in vivo testů s Artemia salina II." Master's thesis, 2015. http://www.nusl.cz/ntk/nusl-332822.
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1 ABSTRACT Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Botany and Ecology Candidate: Beáta Bystrońová Consultant: RNDr. Jitka Vytlačilová, Ph.D. Title of diploma thesis: The evaluation of alkaloids using in vivo tests with Artemia salina II. The most common cause of dementia in the elderly is probably Alzheimer's disease (AD). The prevalence of this disease increases considerably. Nowadays only acetylcholinesterase inhibitors are being used for the treatment of AD, they can relieve symptoms of AD, but can't stop progression of the disease. Consequently there is a need for therapeutic agents against AD, which act on various pathological levels. More intensive recent studies are being carried out on natural substances that could pharmacologically affect AD neurodegenerative processes. Our aim was to carry out the toxicological screening for each tested substance. For the purpose of this work we have used Artemia salina in the experiment which seems to be suitable organism for evaluating acute toxicity. The experiment was conducted in a miniature environment. Four substances which belong to isoquinoline alkaloids: stylopine, tetrahydropalmatine, canadine and scoulerine were tested. The greatest toxicity showed stylopine, slightly lower tetrahydropalmatine and...
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Kvapilová, Radka. "Antiprotozoální aktivita alkaloidů II." Master's thesis, 2015. http://www.nusl.cz/ntk/nusl-334681.
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Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Botany and Ecology Author: Radka Kvapilová Supervisor: RNDr. Jitka Vytlačilová, Ph.D. Title of diploma thesis: Antiprotozoal activity of alkaloids II. The development of new antiprotozoal agents for the treatment of infections is very important. Natural substances can be the source of effective drugs. The aim of this study was to evaluate the antiprotozoal activity of these alkaloids - canadine, scoulerine, tetrahydropalmatine and stylopine. The experiment was conducted on typical model organism Tetrahymena thermophila. Percentage inhibition of the organism was determined using the MTT assay. Subsequently median inhibitory concentration IC50 of the test substances was calculated. From our alkaloids stylopine had the greatest antiprotozoal activity. Antiprotozoal activity decreased in the following order stylopine > canadine > scoulerine > tetrahydropalmatine. Key words: Tetrahymena thermophila, antiprotozoal activity, canadine, scoulerine, tetrahydropalmatine, stylopine
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Balíková, Barbora. "Hodnocení alkaloidů pomocí in vivo testů s Artemia salina I." Master's thesis, 2014. http://www.nusl.cz/ntk/nusl-337408.
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Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Botany and Ecology Candidate: Barbora Balíková Consultant: RNDr. Jitka Vytlačilová, Ph.D. Title of diploma thesis: The evaluation of alkaloids using in vivo tests with Artemia salina I. Alzheimer's disease is the most common cause of dementia and it is one of the lifestyle diseases. There is so far available only limited symptomatic treatment and the occurrence of the lifestyle diseases (and thus Alzheimer's disease) is increasing in recent decades. Therefore it is necessary to find new compounds which will be effective in the treatment of this disease. Toxicological screening - which was our task - is the part of the research of each substance. For the evaluation of the acute toxicity appears as a suitable organism brine shrimp Artemia salina, which was used in the experiment for the purposes of this work. The experiment was conducted in a miniaturized environment. There were tested three substances belonged to the isoquinoline alkaloids: californidine, papaverine and morphine. As the most toxic was evaluated alkaloid californidine, alkaloid papaverine had less toxicity. Morphine appeared essentially as nontoxic with using the same methodology and similar concentrations as in the case of californidine...
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Rozkydalová, Lucie. "REZISTENCE MELANOMŮ K LÉČBĚ VINCA ALKALOIDY." Master's thesis, 2013. http://www.nusl.cz/ntk/nusl-328613.
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Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Pharmacology and toxicology Student: Lucie Rozkydalová Supervisor of Diploma thesis: Prof. PharmDr. František Štaud, PhD. Specialized supervisor: Pr. Pierre Cuq PharmD. PhD., Laure-Anaïs Vincent Title of diploma thesis: Differential resistance of melanoma to vinca-alkaloids Malignant melanoma (MM) represents the most dangerous and very aggressive skin tumor with fast development of drug resistance which is the main obstacle in successful treatment of MM. According to previous studies (microarray data analysis), KIT gene, which plays key role in melanoma pathophysiology, was chosen as one of the potential causes of failure of treatment by vinca alkaloids (VAs) because of its complete underexpression in melanoma CAL1 resistant cells (CAL1R-VAs) in comparison with parental cells (CAL1-wt). Moreover, KIT also interacted with NF-κB and cyclin D1-2 proteins involved in chemoresistance of melanoma - inside molecular network built using IPA software. Although KIT underexpression in resistant CAL1 R-VAs cell lines were confirmed (qRTPCR), KIT repression using specific siRNA transfection did not show any effect on in vitro sensibility of CAL1-wt cells to VAs. It signifies that KIT is not directly involved in melanoma resistance...
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Kavková, Zuzana. "Alkaloidy čeledi Amaryllidaceae a jejich analoga jako potenciální léčiva." Master's thesis, 2016. http://www.nusl.cz/ntk/nusl-344086.
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Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Botany and Ecology Candidate: Zuzana Kavková Supervisor: doc. Ing. Lucie Cahlíková, Ph.D. Title of diploma thesis: Alkaloids of family Amaryllidaceae and their analogues as potential drugs The object of this diploma thesis was to prepare derivatives of alkaloids of Amaryllidaceae family and to deal with their biological activity. These alkaloids are famous for their antibacterial, antiinfectives, antifungal, antimalarial and inhibitory activity against AChE, BuChE and POP and also for cytotoxic effect against cell lines. In the current studies about anticancer activity it was found that the most active alkaloids are Amaryllidaceae alkaloids of these types: lycorine, crinane and pancratistatine. Their biological activity relates closely with their structure. The changes of different parts of the structure can explain the relationship between structure and activity, and also the importance of their organization which is necessary for starting the activity. Based on this finding were for the experiments chosen alkaloids like haemanthamine, haemanthidine and lycorine. An eleven derivatives were prepared and identified mostly by GC-MS and NMR. These derivatives were tested on a wide spectrum of tumor lines....
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Fantová, Adéla. "Alkaloidy - výukové materiály pro SŠ." Master's thesis, 2016. http://www.nusl.cz/ntk/nusl-343041.
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Alkaloids are important natural substances, which are not directly mentioned within the Chemistry Curriculum in the Framework Education Programme for Secondary General Education (Grammar Schools). However, they are a topic which unites more disciplines and allows educating in wider context and across different subjects (Chemistry, Biology and Health Education). They are certainly important topic in terms of drug abuse prevention and Health Education. The objective of this diploma thesis is creation of new educational materials for this topic for grammar school teachers and students. The theoretical part contains a literary research consisting of an analysis of curricular documents, a selection of secondary school chemistry textbooks, a selection of electronic teaching materials, and a proposal for including the topic in grammar school education. Furthermore, it contains a chapter dealing with the issues of drug abuse and its prevention. Research has been conducted by a questionnaire survey on the teaching practice of the topic at grammar schools in the Czech Republic in the practical part. The main output of this diploma thesis is a collection of educational materials on the given topic (PowerPoint presentations, textbook, projects, worksheet, instruction for laboratory exercise, didactic test).
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Jílek, Lukáš. "Biologická aktivita sekundárních metabolitů rostlin II. Alkaloidy Narcissus jonquilla L." Master's thesis, 2015. http://www.nusl.cz/ntk/nusl-379183.
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Jílek L.: The biological activity of secondary plants metabolites II. Alkaloids of Narcissus jonquilla L. Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany and Ecology, Hradec Králové 2015, pp. 74. The aim of the diploma thesis was a preparation of alkaloid extracts to identification of alkaloid patterns and measure cholinesterase inhibitory activity. This activity is useful for treating Alzheimer's disease. Alkaloid extracts of seven Narcissus jonquilla L. (Amaryllidaceae) varieties (Bella Estrella, Bell Song, Fruit Cup, Hill Star, Chit Chat, Martinette, Dick Sickel) were studied with respect to their acetylcholinesterase (HuAChE) and butyrylcholinesterase (HuBuChE) inhibitory activity and alkaloid patterns. Thirteen different alkaloids were identified from their mass spectra and retention times. All samples exhibited content of tazettine, most samples contained lycoramine and galanthamine. Promising HuAChE inhibition activity was demonstrated by Narcissus jonquilla L. cv. Bell Song with IC50 values of 6,19 ± 0,85 μg/mL. The strongest inhibitory activity against HuBuChE was detected in extract from Narcissus jonquilla L. cv. Bella Estrella with IC50 value of 18,39 ± 1,51 μg/mL. Keywords: Alzheimer's disease, Amaryllidaceae, Narcissus, GC/MS,...
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Nováková, Dana. "Biologická aktivita sekundárních metabolitů rostlin I. Alkaloidy Narcissus jonquilla L." Master's thesis, 2015. http://www.nusl.cz/ntk/nusl-331210.
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Nováková D.: Biological activity of secondary plants metabolites I. Alkaloids of Narcissus jonquilla L. Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany and Ecology, Hradec Králové 2015, pp. 70. The aim of the diploma thesis was a preparation of alkaloid extracts to identification of alkaloid patterns and measure cholinesterase inhibitory activity. This activity is useful for treating Alzheimer's disease. Alkaloid extracts of seven Narcissus jonquilla L. (Amaryllidaceae) varieties (Sundial, Sundisc, Sweetness, Waterperry, Simplex, Twinkling Yellow, Yazz) were studied with respect to their acetylcholinesterase (HuAChE) and butyrylcholinesterase (HuBuChE) inhibitory activity and alkaloid patterns. Twenty-three alkaloids were determined by GC/MS, and ten of them identified from their mass spectra and retention times. All samples exhibited content of galanthamine, most samples contained lycorine and tazettine. Promising HuAChE inhibition activity was demonstrated by Narcissus jonquilla L. cv. Waterperry with IC50 values of 6.53 ± 0.88 μg/mL. The strongest inhibitory activity against HuBuChE was detected in extract from Narcissus jonquilla L. cv. Sundisc with IC50 value of 5.09 ± 0.64 μg/mL. Keywords: Alzheimer's disease, Amaryllidaceae, Narcissus,...
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Panchartková, Markéta. "Biologická aktivita sekundárních metabolitů rostlin III. Alkaloidy Narcissus tazetta L." Master's thesis, 2015. http://www.nusl.cz/ntk/nusl-331236.
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Panchartková, M.: Biological aktivity of secondary plants metabolites III. Alkaloids of Narcissus tazetta L., Diploma thesis, Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany and Ecology, Hradec Králové, 2015, 67s. Plants from the Amaryllidaceae family contain alkaloids that have multiple biological effects. There is described antiviral, antitumor, antibacterial, antimalarial and anti-fungal effect. Activity against human cholinesterases is important too. The aim of this thesis was to prepare seven alkaloid extracts of individual cultivars of the plants Narcissus and then to realize their GC/MS analysis. Thanks to this analysis, several different structural types of alkaloids from the Amaryllidaceae family were identified. The most frequently identified alkaloids were homolycorine, lycorine, tazettine and galanthamine type. This was followed by the measuring of biological activity against human acetylcholinesterase (HuAChE) and butyrylcholinesterase (HuBuChE). The highest inhibitory activity IC50 identified the alkaloidal extract of the Narcissus jonquilla cv. New baby with the values in relation to HuAChE 13,78 ± 1,48 and in relation to HuBuChE 96,12 ± 9,55. The main reason was probably the highest content of galanthamine of all cultivars,...
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Kohelová, Eliška. "Alkaloidy čeledi Amaryllidaceae: isolace, strukturní identifikace, biologická aktivita. II." Master's thesis, 2017. http://www.nusl.cz/ntk/nusl-379168.
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Kohelová E: Alkaloids of Amaryllidaceae family: isolation, structural identification, biological activity. II Diploma thesis, Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany and Ecology, Hradec Králové, 2017, 77p. The aim of the diploma thesis was a preparation of alkaloidal extract from fresh bulbs of Narcissus cv. PROFESSOR EINSTEIN to izolate two Amaryllidaceae alkaloids by column and thin layer chromatography. Subsequently these alkaloids were subjected to structural MS and NMR analysis and tested for biological activity against human cholinesterases (HuAChE and HuBuChE) and for cytotoxic activity. In cooperation with the Faculty of Agrobiology, Food and Natural Resources, Czech University of Life Sciences Prague, antifungal and antimicrobial activities of alkaloids were tested, and in cooperation with Faculdade de Medicina da Universidade de Lisboa Portugal antimalarial activity of alkaloids was studied. Isolated substances were identified as galanthamine, caranine and pluviine. Pluviine was isolated in an amount allowing only structural analysis. In the test for determining cholinesterase inhibitory activity of caranine the following values were obtained: IC50, HuAChE = 320 ± 42 μM a IC50, HuBuChE = 486 ± 56 μM. Galanthamine (IC50,...
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Černá, Kateřina. "Alkaloidy čeledi Amaryllidaceae: isolace, strukturní identifikace, biologická aktivita. IV." Master's thesis, 2019. http://www.nusl.cz/ntk/nusl-405164.
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Perennial plants from the Amaryllidaceae family are generally known for their beauty but also like herbs which contain wide range of alkaloids. To these days more than 500 alkaloids have been isolated. Amaryllidaceae alkaloids (AmA) are derivatived from aminoacid tyrosine and divided into nine basic groups. Biological activity of these substances icludes antitumor, antibacterial, antifungal, antiviral, antimalarial activity and some of them are used for treatment Alzheimer's disease (AD). Narcissus cv. PROFESSOR EINSTEIN have been choosen thanks to previous research of summary extract. Twelve alkaloids have been detected by GC-MS and ten of them have been identified (e.g.: lykoramine, pluviine, haemanthamine, pancracine, homolycorine). Due to this diversity of alkaloids and the fact that summary extract has relatively high inhibitory activity (IC50 = 49,99 ± 5,38 μg/mL) against HuBuChE Narcissus have been appropriate for isolation of the alkaloids and for further study of their biological activity. Summary ethanolic extract for gain pure compounds was prepared from 34.3 kg fresh bulbs. Separation was initiated by column chromatography and extract was divided into almost 500 fractions. Some of them were put together owing to TLC analysis and finally 27 subfractions were formed. Subfraction Nr. 26...
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Hanusová, Petra. "Alkaloidy čeledi Amaryllidaceae: isolace, strukturní identifikace, biologická aktivita. III." Master's thesis, 2017. http://www.nusl.cz/ntk/nusl-361790.
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Hanusová P.: Alkaloids of Amaryllidaceae family: isolation, structural identification, biological activity. III. Diploma thesis, Charles University, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany and Ecology, Hradec Králové, 2017. For phytochemical study was selected plant cultivar Narcissus cv. PROFESSOR EINSTEIN. The aim of the work was to isolate Amaryllidaceae alkaloids in pure form and screening of their biological activities. Summary alkaloidal extract was prepared from 34 kg of fresh bulbs and separated by column chromatography. Preparative TLC and crystallization were used for the isolation of substances from subfraction 6/1. Two pure alkaloids of galanthamine structural type were obtained. The alkaloids were identified based on their MS, NMR analysis and optical rotation as narwedine and lycoraminone. Lycoraminone has been isolated for the first time from natural source. Both substances were tested for their acetylcholinesterase, butyrylcholinestease and prolyl oligopeptidase inhibition activity. Anticancer activity against two gastrointestinal cancer cell lines Caco-2 and HT-29 (colorectal adenocarcinoma) and antimalarial activity has been also measured. Unfortunately, none of isolated alkaloids showed some significant activity in biological assays. Keywords:...
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Dohnalová, Alice. "Alkaloidy čeledi Amaryllidaceae: isolace, strukturní identifikace, biologická aktivita. I." Master's thesis, 2017. http://www.nusl.cz/ntk/nusl-361794.
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Dohnalova A: Alkaloids of Amaryllidaceae family: isolation, structural identification, biological activity. I; Diploma thesis, Charles University, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany and Ecology, Hradec Králové, 2017, 64 p. The Amaryllidaceae family includes bulbous, beautifully flowering plants that have been used for thousands of years in traditional medicine. The major chemical compounds found in this particular plant family are alkaloids, namely Amaryllidaceae alkaloids. Until now, more than 500 isoquinoline alkaloids have been discovered, which exhibit a diverse biological activity including antitumor and antibacterial. They are also able to inhibit acetylcholinesterase. The aim of the diploma thesis was to process 34 kg of fresh bulbs of Narcissus cv. PROFESSOR EINSTEIN and to prepare an alkaloidal extract. This extract was further divided by column chromatography to almost 500 fractions which were merged based on TLC into 27 subfractions. The subfractione No. 17 was selected for isolation of at least one pure alkaloid. Preparative TLC was used for the the isolation. One pure compound was obtained in crystalic form which was then subjected to structural analysis by EI-MS and NMR methods. Further studies of biological activities were performed in...
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Tkáčová, Beáta. "Alkaloidy kultivarů rodu Narcissus a jejich biologická aktivita I." Master's thesis, 2020. http://www.nusl.cz/ntk/nusl-435188.
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Charles University, Faculty of Pharmacy in Hradec Králové Department: Department of Pharmaceutical Botany (16-16130) Author: Tkáčová Beáta Supervisor: PharmDr. Kateřina Breiterová, Ph.D. Title of thesis: Alkaloids of Narcissus species cultivars and their biological activity I. Key words: Narcissus, alkaloids, biological activity, Alzheimer's disease. The main aim of this diploma thesis was to obtain summary alkaloid extracts from bulbs of five species cultivars (Narcissus cv. Acropolis, Delta, White Marvel, Kedron, Scarlet Gem) and one variety (Narcissus albus var. plenus odoratus), labeled as AL-450, AL-457, AL-460, AL-463, AL-467 and AL-508, from which samples were subsequently prepared for GC-MS analysis and screening of biological activities (cholinesterase inhibitory activity and cytotoxicity). Totally, 18 alkaloids were identified by GC-MS analysis, comparing their mass spectra. Identified alkaloids include 3-O-demethylmaritidine, 11,12-dehydroanhydrolycorine, assoanine, dehydroassoanine, galanthamine, galanthine, haemanthamine, hippeastrine, incartine, lycoramine, lycorine, narwedine, norpluvine, pancracine, pluvine, pseudolycorine and tazettine. Samples of cultivars AL-457, AL-460, AL-463 and AL-508, showed relatively promising hAChE inhibitory activity in screening assay (c = 50 µg/ml),...
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Al, Shammari Latifah Ajaj M. "Alkaloidy rodu Hippeastrum (Amaryllidaceae): izolace, strukturní identifikace, biologická aktivita." Doctoral thesis, 2021. http://www.nusl.cz/ntk/nusl-445960.
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Charles University in Prague, Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Botany Candidate: MSc. Latifah Al Shammari Supervisor: Prof. Ing. Lucie Cahlíková, Ph.D. Title of Doctoral Thesis: Alkaloids of the genus Hippeastrum (Amaryllidaceae): isolation, identification, biological activity. Hippeastrum x hybridum cv. Ferrari was chosen based on results of previous screening studies for detailed phytochemical study for the purpose of isolation of the widest range of AAs. From 25 kg of fresh bulbs was obtained 29,46 g of purified alkaloidal extract, which was processed using column chromatography. Finally, 18 pure alkaloids were isolated including one new homolycorine-type alkaloid (9-O-demethyllycorenine). All compounds were identified by spectrometric techniques (GC-MS, ESI-MS, NMR, optical rotation) and by comparison with literature data. All alkaloids, isolated in sufficient amount, were tested for their biological activities associated with Alzheimer's disease (inhibition of hAChE, hBuChE, and POP), and cytotoxic activity. The inhibitory activity against human cholinesterases was determined in vitro by a modified Ellmanʼs spectrophotometric method. In the hAChE/hBuChE assay, except for 1,2- O,O'-diacetyl-dihydrolycorine which demonstrated a mild hBuChE inhibition potency...
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Mišáková, Kamila. "Alkaloidy rostlin čeledi Amaryllidaceae a jejich biologická aktivita 1." Master's thesis, 2014. http://www.nusl.cz/ntk/nusl-333192.
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Mišáková K: Alkaloids of the Amaryllidaceae family and their biological activity 1. Diploma thesis, Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany and Ecology, Hradec Králové, 2014, 63 p. The aim of the diploma thesis was a preparation of alkaloidal extract from Nerine Bowdenii to izolation of 2 pure alkaloids by column and thin layer chromatography. Subsequently these two alkaloids were subjected to structural MS and NMR analysis and tested for biological activity against human cholinesterases (HuAChE and HuBuChE) and for antioxidant and cytotoxic activity. Isolated substances were identified as ambelline and undulatine alkaloids, which have been already described previously in this plant. In the test for determining cholinesterase inhibitory activity of ambelline and undulatine the following values were measured; for ambelline: IC50, HuAChE = 169 ± 7 μM a IC50, HuBuChE = 985 ± 25 μM, for undulatine: IC50, HuAChE = 23,52 ± 1,19 μM a IC50, HuBuChE > 1000 μM. Galanthamin (IC50, HuAChE = 1,71 ± 0,007 μM, IC50, HuBuChE = 42,30± 1,30 μM), huperzin A (IC50, HuAChE = 0,033 ± 0,001 μM, IC50, HuBuChE > 1000 μM) and eserin (IC50, HuAChE = 0,063 ± 0,001 μM, IC50, HuBuChE = 0,130 ± 0,004 μM) were used like a positive controls. In the test for...
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Jeřábková, Lenka. "Inhibice lidského rekombinantního CYP2D6 isochinolinovými alkaloidy." Master's thesis, 2010. http://www.nusl.cz/ntk/nusl-299241.
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The purpose of this work was to screen a set of isoquinoline alkaloids for their inhibitory potency toward CYP450 isoenzyme CYP2D6. Since the human cytochrome P450 plays a pivotal role in a metabolism of both xenobiotics and endogenous substances, studying its interactions is a basic task in early drug development. CYP2D6 is due to its high polymorphism monitored very often. The in vitro method with fluorometric detection was used to determine the inhibitory effect of 20 alkaloids towards the recombinant human CYP2D6. Isoquinoline alkaloids were divided into the groups based on their relative structures. It was determined that 11 out of 20 are potent inhibitors, 3 moderate, 5 weak and one is not inhibitor. In percentage representation it means that 70% of all measured compounds are at least moderate potent inhibitors to CYP2D6 in this assay. They create mainly the members of protoberberine alkaloid group. The structure of these compounds might contribute to the searching of new inhibitors for data-sets for in silico drug metabolism predicting methods.
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Marečková, Lucie. "Biologická aktivita sekundárních metabolitů rostlin VII. Alkaloidy Vinca minor L." Master's thesis, 2018. http://www.nusl.cz/ntk/nusl-387897.
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Marečková, L .: Biological activity of secondary plant metabolites VII. Alkaloids of Vinca minor L. Diploma thesis, Charles University, Faculty of Pharmacy in Hradec Kralove, Hradec Králové, Department of pharmaceutical botany and ecology, Hradec Králové 2018 There was prepared an extract from aerial parts of the plant Vinca minor L. This prepared extract was separated by the column chromatography into individual fractions. One chosen fraction was separated by TLC on silicagel. Two substances were isolated and they we identified by GC/MS and NMR as (-)-minovin and (+)-minovincin. These two substances were tested for their inhibition activity against human acetylcholinesterase (hemolysate of human erythrocytes) and butyrylcholinesterase (human plasma). Their inhibition activity was compared to standards which were Galanthamin, Huperzin A and Eserin. (+)-Minovincin did not show significant inhibitory activity against either enzyme (IC50 = AchE > 1000 µM, BuChE 655,05 ± 35,37 µM) and it is not suitable for further investigation. (-)-Minovin showed no significant activity against AChE (IC50 = 234,27 ± 63,40 µM), activity against BuChE (IC50 = 26,32 ± 2,52 µM) was higher than inhibitory akctivity of Galanthamin, but still relatively low for further investigation. The aim of this work was mainly the...
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Klíčová, Anna. "Alkaloidy dřeva druhu Liriodendron tulipifera L. a jejich biologická aktivita." Master's thesis, 2018. http://www.nusl.cz/ntk/nusl-388858.
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Klíčová A.: Alkaloids from wood of the species Liriodendron tulipifera L. and their biological activity. Diploma thesis, Charles University, Faculty of Pharmacy in Hradec Králové, Department: Pharmaceutical Botany, Hradec Králové, 2018. Supervisor: PharmDr. Anna Hošťálková, Ph.D. Key words: Liriodendron tulipifera, secondary metabolites, alkaloids, biological activity Alzheimer's disease (AD) is the most common type of dementia. It is neurodegenerative disorder. Patients suffer from cognitive disorder in combination with aphasia, apraxia or disorders of executive functions, which leads to exacerbation of working or social skills. Nowadays, there exist no casual treatment for AD, and that is why the intense research is still waging. Currently there are available remedies, which can slow down progress of AD. These drugs includes also natural substances. An alkaloid extract of Liriodendron tulipifera L. wood showed promising inhibition of human cholinesterases in a preliminary testing. These results were the reason why this extract has been chosen for further isolation of single alkaloids and identification of their biological activity. Isolation was made by column chromatography with step gradient elution. Then was used preparative TLC to isolate single alkaloids. Identification of alkaloids was...
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Šípková, Pavla. "Biologická aktivita sekundárních metabolitů rostlin X. Alkaloidy Vinca minor L." Master's thesis, 2019. http://www.nusl.cz/ntk/nusl-403954.
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Šípková, P.: Biological activity of secondary plants metabolites X. Alkaloids of Vinca minor L. Diploma thesis, Charles University, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany, Hradec Králové, 2019, 66 s. Key words: Apocynaceae, Vinca minor, alkaloids, isolation, biological activity, screening Alzheimer's disease is a progressive neurodegenerative disease. The number of affected patients is constantly increasing. This disease cannot be treated casually, therefore discovering and testing new substances that could potentially be used in a treatment is very important. The Vinca minor L. fraction after column chromatography was separated by flash chromatography. Isolation of the individual alkaloids was performed by preparative TLC. Based on NMR and MS analyses and comparison with literature, alkaloids were identified as vincarubine and (-)-vinoxine. Modified Ellman's method was used to test cholinesterase inhibitory activity of isolated alkaloids. Acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) are enzymes, that play a very important role in the pathofysiology of Alzheimer's diasease. (-)-Vinoxine showed relatively high activity against BuChE (IC50 = 24,61 ± 1,71 µM), inhibitory activity against AChE was insignificant (IC50 > 1000µM). Vincarubin did not...
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Bouz, Lukáš. "Biologická aktivita sekundárních metabolitů rostlin V. Alkaloidy Vinca minor L." Master's thesis, 2016. http://www.nusl.cz/ntk/nusl-344091.
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Bouz L.: Biological activity of secondary plants metabolites V. Alkaloids of Vinca minor L. Diploma thesis, Charles University, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany and Ecology, Hradec Králové 2016. Summary extract obtained from dried aerial parts of Vinca minor L. was separated by column chromatography with petrol, chloroform and ethanol to 531 fractions. By further separation of fractions, following preparative thin layer chromatography and crystallization 2 alkaloidal compounds marked LB-2 and LB-3 were isolated. These compounds were identified by GC/MS, 1 H- and 13 C-NMR spectroscopy and by use of physical-chemical methods. The structure of compounds were elucidated as indole alkaloids (+)-vincaminoreine (LB-2) and (+)-vincamine (LB-3). Both substances were tested for their inhibition activity against human cholinesterases. (+)-Vincamine didn't exhibited in comparison with standard drugs (galanthamine IC50 AChE: 1,710 ± 0,065 µM, IC50 BChE: 42,30 ± 1,30 µM; huperzine A IC50 AChE: 0,033 ± 0,001 µM) any inhibition activity. On the other hand (+)-vincaminoreine exhibited fairly strong selective inhibition of BChE (IC50 = 8,71 ± 0,49 µM) with no inhibition of AChE. Key words: Vinca minor L., indole alkaloids, vincamine, vincaminoreine, Alzheimer disease,...
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Vítovcová, Aneta. "Biologická aktivita sekundárních metabolitů rostlin IV. Alkaloidy Vinca minor L." Master's thesis, 2016. http://www.nusl.cz/ntk/nusl-347048.
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Vítovcová, A.: Biological activity of secondary plants metabolites IV. Alkaloids of Vinca minor L. Diploma thesis, Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany and Ecology, Hradec Králové 2016. Extract of Vinca minor L. was separated to fractions in column chromatography. Flash chromatography, preparative TLC and crystalisation led to isolation of two alkaloids from fraction number two and number five. Alkaloids were identified by GC/MS as (+)-vincaminorine and vincorine. These alkaloids were tested for their inhibition activity towards cholinesterase (AChE and BuChe). Obtained activities IC50 were compared with standards (galanthamine, huperzine A). The most interesting activity against galanthamine (AChE 1,710 ± 0,065 µM, BuChE 42,30 ± 1,30 µM) and huperzine A (AChE 0,033 ± 0,001 µM, BuChE > 1000 µM) showed vincorine (AChE > 1000 µM, BuChE 9,75 ± 0,45 µM). His activity toward BuChE is higher than the activity of both standards. Inhibition activities of (+)-vincaminorine (AChE 746,5 ± 84,13 µM, BuChE 684,32 ± 70,66 µM) are negligible. Key words: Alzheimerʼs disease, cholinesterase, Apocynaceae, Vinca minor L., indole alkaloids
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Kučerová, Jana. "Biologická aktivita sekundárních metabolitů rostlin VI. Alkaloidy Vinca minor L." Master's thesis, 2016. http://www.nusl.cz/ntk/nusl-347054.
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1 ABSTRACT Kučerová J.: Biological activity of secondary plants metabolites VI. Alkaloids of Vinca minor L. Diploma thesis, Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of pharmaceutical botany and ecology, Hradec Králové 2016, 67 pages. Isolation of alkaloids was done from extract of Vinca minor, family Apocynaceae. Individual substances obtained were examined for their ability to inhibit human acetylcholinesterase and butyrylcholinesterase. The basic extract was after an initial extraction with 95% ethanol pre-purified by extraction with chloroform. This chloroform extract was divided further by column chromatography on a total of 531 fractions. The fractions obtained were, based on the similarities identified by thin layer chromatography, interconnected in a final number of 17 fractions. The mobile phase for column chromatography were mixtures of chloroform and medical gasoline, chloroform and ethanol, and ethanol itself. For further testing were used fractions number 2 and 5. From the fraction 2 was by preparative thin layer chromatography and subsequent crystallization isolated substance number 1. After analysis of this substance by GC/MS was found that it is a (+) - vincaminorein. Further was examined it's biological activity towards cholinesterases, which found a...
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Veselá, Tereza. "Vliv biologické ochrany rostlin na produkci sekundárních metabolitů Papaver somniferum IV." Master's thesis, 2018. http://www.nusl.cz/ntk/nusl-387760.
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Vesela T.: Influence of plant biological control on production of secondary metabolites of Papaver somniferum IV. Diploma thesis, Charles University, Faculty of Pharmacy in Hradec Kralove, Department of pharmaceutical botany, Hradec Kralove 2018. In the experimental part of the thesis was studied the influence of plant biological control on the production of the main pharmaceutically usable secondary metabolites of opium poppy (Papaver somniferum L.). The contents of alkaloids morphine, codeine, thebain, papaverine and narcotine were monitored in the capsules and stems. Two poppy varieties, Orbis and Lazur, were selected for the experiment. Half of the plots were treated with the fungicidal biopreparate Polyversum, containing the germinable spores of oomycete Pythium oligandrum. Pythium oligandrum directly attacks the fungal pathogens. It also uses indirect control mechanisms, induces resistance in plants and promotes their growth. The remaining untreated plots served as a reference check. The extract was prepared from the individual samples. Subsequent analysis was performed using high performance liquid chromatography. The results show no positive effect of treatment on the content of all quantified alkaloids in poppy straw. Biosynthesis of alkaloids and Pythium oligandrum activity can be...
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Šilhová, Markéta. "Interakce alkaloidů s přechodnými kovy II." Master's thesis, 2019. http://www.nusl.cz/ntk/nusl-405336.
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Charles University, Faculty of Pharmacy in Hradec Králové Department of: Pharmaceutical Botany Consultant: Ing. Kateřina Macáková, Ph. D. Student: Markéta Šilhová Title of Thesis: Interactions of alkaloids with transition metals II. Copper is an important component of the human body. It is involved in the right functioning of organ systems and is also a part of many important body enzymes. It is necessary to maintain a balanced amount of copper in the body in order to avoid excess or deficiency, which can lead to various diseases. The aim of this diploma thesis was to determine the copper chelating and copper reducing effects of isoquinoline alkaloids berberine chloride, canadine, corydaline, sculerine, sinactine, stylopine, tetrahydropalmatine, allocryptopine, protopine, corycavamine and cryptopine. In experimental measurements the determination of chelation of copper ions with hemytoxyline and the determination of chelation and reduction of copper ions using disodium salt of bathocuproindisulfonic acid was performed. The highest reducing activity was exhibited by scoulerine, whose structure in comparison with other alkaloids contains hydroxyl groups and which has been exhibited in the past to inhibit the growth of tumour cell. The lowest reducing activity was measured for protopine alkaloids and...
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Rzepecká, Radka. "Interakce alkaloidů s přechodnými kovy I." Master's thesis, 2019. http://www.nusl.cz/ntk/nusl-405499.
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Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Botany Candidate: Radka Rzepecká Supervisor: Ing. Kateřina Macáková, Ph.D. Title of Thesis: Interactions of alkaloids with transition metals I. Copper is one of the essential trace elements that are necessary for the proper functioning of the organism. Copper is a significant component of many enzymes that affect various metabolic processes in the human body. It is important that the level of copper in the body is regulated because its deficit or excess lead to a variety of pathological conditions. Alkaloids are secondary plant metabolites that are distinguished by numerous biological activities. In this thesis the copper-chelating and copper-reducing activity of eleven isoquinoline alkaloids was measured: boldine, isocorydine, (+)-bulbocapnine, (+)-corydine, glaucine, (-)-sinoacutine, (-)-californidine, (-)-escholtzine, platycerine, (-)-fumaricine, and (+)- parfumine. Alkaloid activity was measured at four (patho) physiological pH values by a verified spectrophotometric method using two indicators: bathocuproinedisulfonic acid disodium salt and hematoxylin. Based on the results, structure-effect relationships were derived. The results show that none of the tested substances was able to chelate copper ions. In...
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Dočekalová, Linda. "Železo-chelatační aktivita vybraných alkaloidů III." Master's thesis, 2016. http://www.nusl.cz/ntk/nusl-347995.
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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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Schickerová, Julie. "Alkaloidy Narcissus pseudonarcissus cv. Dutch Master: isolace, strukturní identifikace, příprava analog, biologická aktivita." Master's thesis, 2018. http://www.nusl.cz/ntk/nusl-387900.
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Schickerová Julie: Alkaloids of Narcissus pseudonarcissus cv. Dutch Master: isolation, structural identification, preparation of analogues, biological activity. Diploma thesis, Charles University, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany, Hradec Králové, 2018, 73 p. The purpose of this diploma thesis was to isolate the substances from the fraction ND 15- 9, which was obtained by column chromatography of the alkaloid extract of Narcissus pseudonarcissus cv. Dutch Master. The method of preparative TLC was used to separate this fraction, and the three purified compounds were isolated in the pure state NDS1-NDS3. NMR, GC/MS and optical rotation were used to determine their structure. The obtained data were compared with data in the literature and further studies on their biological activity were performed. Isolated substances were identified as epimaritidine, crinine and tetrahydromasonine. Their inhibitory activities (IC50, AChE > 1000 μM, IC50, BuChE > 1000 μM) versus human erythrocyte AChE and plasma BuChE were inactive compared to galanthamine standards (IC50, AChE = 1.71 ± 0.07 μM, IC50, BuChE = 42.30 ± 0.10 μM), huperzin A standards (IC50, AChE = 0.033 ± 0.001 μM, IC50, BuChE > 1000 μM) and berberin standards (IC50, AChE = 0.71 ± 0.01 μM, IC50, BuChE = 30.7 ± 3.5...
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Tanková, Sabina. "Alkaloidy rodu Narcissus a jejich biologická aktivita." Master's thesis, 2019. http://www.nusl.cz/ntk/nusl-396795.
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Charles University, Faculty of Pharmacy in Hradec Králové Department of Pharmacognosy Candidate: Sabina Tanková Supervisor: PharmDr. Daniela Hulcová, PhD. Title of diploma thesis: Alkaloids of the genus Narcissus and their biological activity. Key worlds: Narcissus pseudonarcissus L. cv. Dutch Master, Amaryllidaceae, alkaloids, AChE, BuChE, POP, GSK-3β, biological activity. Alkaloid extract obtained from bulbs of Narcissus pseudonarcissus L. cv. Dutch Master was extracted by ethanol and was purified by liquid-liquid extraction and fractionated by column chromatography to individual fractions. At the end, were obtained 11 pooled fractions, which were used to isolate pure alkaloids. The ND 3-5 / 7 fraction was processed by preparative thin layer chromatography followed by crystallization of pure substances. In total, 5 alkaloid substances of ST1D2, ST1D3, ST2A, ST2B1 and ST3C were obtained from this fraction in various amounts. These substances were determined by GC-MS analysis, NMR analysis and optical rotation. Subsequently, the obtained data were compared with the NIST library spectra and the literature. Isolated substances have been identified as caranine, O-ethyllycorenine, narwedine, pluviine and N-demethylhomolycorine. The alkaloids obtained in sufficient amounts were subsequently subjected to...
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Potůčková, Adéla. "Deriváty Amaryllidaceae alkaloidů a jejich biologická aktivita." Master's thesis, 2020. http://www.nusl.cz/ntk/nusl-412219.
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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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Puskásová, Dominika. "Alkaloidy čeledi Amaryllidaceae a jejich biologická aktivita I." Master's thesis, 2019. http://www.nusl.cz/ntk/nusl-397381.
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Puskásová Dominika: Alkaloids of the Amaryllidaceae family and their biological activity I. Diploma thesis 2019. Charles university in Prague, Faculty of Pharmacy in Hradec Králové, Department of Pharmacognosy. The aim of this thesis was to isolate alkaloids from herbal extract, which was obtained from Narcissus pseudonarcissus 'Dutch Master' plant. The preparation and column chromatography of the extract were performed by PharmDr. Daniela Hulcová, Ph.D. as a part of her doctoral study. Using the preparative TLC method, 2 alkaloids marked as No.2.1 and 2.2.2 were isolated from the fraction No.4. Their structure was determined by using the NMR, GC-MS analysis and optical rotation. After comparing the data obtained with literature, the compounds were identified as (+)-homolycorine and (+)-masonine. Both homolycorine and masonine were subsequently subject to testing of inhibitory activity against acetylcholinesterase (AChE), butyrylcholinesterase (BuChE), prolyloligopeptidase (POP) and glycogensynthase kinase 3β (GSK-3β). The activity was expressed as IC50 and was compared to IC50 of the reference substances. Galanthamine (IC50 AChE = 1,7 ± 0,1 μM, IC50 BuChE = 42,3 ± 1,3 μM) and huperzine A (IC50 AChE = 0,033 ± 0,001 μM, IC50 BuChE > 500 μM) were used as standards to compare the inhibitory activity...
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Kosturko, Štefan. "Alkaloidy čeledi Amaryllidaceae a jejich biologická aktivita II." Master's thesis, 2020. http://www.nusl.cz/ntk/nusl-435016.
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Charles University, Faculty of Pharmacy in Hradec Králové Department: Department of Pharmacognosy (16-16180) Author: Štefan Kosturko Supervisor: PharmDr. Marcela Šafratová, Ph.D. Advisor: PharmDr. Daniela Hulcová, Ph.D. Thesis title: Alkaloids of the family Amaryllidaceae and their biological activity II. Key words: Narcissus pseudonarcissus dutch master; bulbs; alkaloidal extracts; GC/MS analysis; biological activity; acetylcholinesterase; butyrylcholinesterase. The main aim of the thesis ‚,Alkaloids of the family Amaryllidaceae and their biological activity II.'' was the isolation of alkaloids, as a pure substances, in sufficient quantities to identify their structure and to test their biological aktivity in vitro. Alkaloids were separated from subfraction number 82 - 97 of weigh 2,3268 g. This subfraction was a part of the total plant extract, which was prepared by PharmDr. Daniela Hulcová Ph.D., as a part of her dissertation thesis and who also performed primary extraction and separation work. A total and concentrated alkaloid extract weighing 58 g, which included the aforementioned subfraction, was obtained. The already mentioned alkaloid subfraction, was divided by preparative thin-layer chromatography into five separates, which were subjected to further phytochemical work, and five pure...
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Loskotová, Lenka. "Interakce alkaloidů s přechodnými kovy IV." Master's thesis, 2020. http://www.nusl.cz/ntk/nusl-412235.
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Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Botany Candidate: Bc. Lenka Loskotová Supervisor: doc. Ing. Kateřina Macáková, Ph.D. Title of Thesis: Interactions of alkaloids with transition metals IV. Copper is a biogenic trace element that participates in the proper function of an organism. It is part of a number of enzymes and participates in metabolic processes in the human body. The level of copper in the organism should be regulated to avoid its excess or deficit, as pathologies could occur. Alkaloids are natural nitrogenous substances of alkaline nature. We find many biological activities in them. The aim of this thesis was to measure copper-chelating and copper- reducing activity of isoquinoline alkaloids: corypalmine, thalictricavine, 8-oxoberberine, fumarilin, norisocorydine and laurotetanine. Alkaloid activity was measured at different pH environments (4.5; 5.5; 6.8 and 7.5) and in the DMSO environment by a spectrophotometric method using hematoxyline and acid disodium salt bathocuproindisulfonic. Based on the results, structure-effect relationships were derived. In experimental measurement, it was found that none of us tested alkaloids showed chelating activity. Reduction activity has been demonstrated in all test substances. The lowest activity...
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Cymbál, Martin. "Interakce alkaloidů s přechodnými kovy III." Master's thesis, 2020. http://www.nusl.cz/ntk/nusl-412276.
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Charles University Pharmaceutical Faculty in Hradec Králové Department of Pharmaceutical Botany Candidate: Bc. Martin Cymbál, DiS. Supervisor: doc. Ing. Kateřina Macáková, Ph.D. Diploma thesis 2019/2020: Interactions of alkaloids with transition metals III., pp. 86. Copper is one of the important trace elements in the body. It regulates various enzymatic pathways. This work monitors the chelating and reducing activity of isochinoline alkaloids of the family Amaryllidaceae. The alkaloids of Amaryllidaceae have a large number of effects such as analgesic, narcotic, antiarrhythmic, antihypertensive, bronchodilatory, chemotherapeutic, antiparasitic, uteretonic, locally anesthetic, mydriatic and many other significant effects. An important representative is galanthamine hydrobromide, which is therapeutically used and is an inhibitor of acetylcholinesterase. Galanthamine type alkaloids (galanthamine, galanthamine hydrobromide, chlidanthine), lycorine type (lycorine, galanthine), haemanthamine type (haemanthnamine, vittatine) and montanine type (montanine) were studied. The methodology of the work was to determine the chelating and reducing activity with the use of the hematoxylin indicator and bathocuproindisulfonic acid, at different pH or in dimethylsulfoxide. Of the alkaloids studied, galanthamine and...
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Hojgrová, Veronika. "Alkaloidy Vinca minor L. a jejich biologická aktivita VIII." Master's thesis, 2021. http://www.nusl.cz/ntk/nusl-446426.
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V. Hojgrová: Alkaloids of Vinca minor L. and their biological activity VIII. Diploma thesis, Charles University, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany. Number of pages 69. This diploma thesis deals with the isolation of alkaloids from Vinca minor L. from the family Apocynaceae. Separation of alkaloids from the selected fraction (VM 215-258) or from their subfractions (VM 34-41, VM 86, VM 87-113) was performed by preparative TLC. Two pure alkaloids were isolated from the subfraction (VH 34-41). The first VH-1 alkaloid not yet isolated and the second VH 2 alkaloid: (-)-raucubainin. Alkaloids were identified by EI-MS, LC-MS, NMR and optical rotation and were compared with data in the literature. Isolated alkaloids were tested for acetylcholinesterase (AChE), butyrylcholinesterase (BuChE) and prolyloligopeptidase (POP) inhibitory activity and for cytotoxicity. Both substances did not show significant cholinesterase inhibitory activity IC50 against AChE after measurement, only (-)-raucubainin showed a slight activity against BuChE (IC50 = 94 ± 7 μM), VH-1 was found to be inactive (IC50 > 100 μM). POP inhibitory activity has so far only been tested for (-)-raucubainin; was found to be inactive (IC50 > 1000 µM). The results of the cytotoxic activity of the alkaloids...
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Breiterová, Kateřina. "Alkaloidy rostlin čeledi Amaryllidaceae jako potenciální léčiva v terapii civilizačních onemocnění." Doctoral thesis, 2019. http://www.nusl.cz/ntk/nusl-398631.
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Charles University, Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Botany Candidate: Mgr. Kateřina Breiterová Supervisor: Assoc. prof. Ing. Lucie Cahlíková PhD. Title of Doctoral Thesis: Alkaloids of the Amaryllidaceae family as potential drugs in therapy of diseases of affluence Key words: alkaloids, Amaryllidaceae, analogues, AChE, BuChE, POP, GSK-3β, cell cycle progression, apoptosis Narcissus cv. Professor Einstein was chosen based on results of previous screening studies for detailed phytochemical work for the purpose of isolation of the widest range of AmA. From 34,3 kg of fresh bulbs was obtained 31,7 g of purified alkaloidal extract, which was processed using column chromatography with stepwise elution by light petrol, chloroform and ethanol in different ratios to almost 500 fractions. These fractions were fused into 27 subfractions, which were processed by preparative TLC, vacuum column chromatography and crystallization. Finally, 25 pure alkaloids were isolated. All compounds were identified by GC-MS, ESI-MS, NMR, optical rotation and literature. One compound was identified as a new unpublished alkaloid of lycorine structure type. All alkaloids isolated in sufficient amount were tested for their biological activities associated with Alzheimer's disease (inhibition of...
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Pavuková, Simona. "Alkaloidy Vinca minor L. a ich biologická aktivita II." Master's thesis, 2021. http://www.nusl.cz/ntk/nusl-446421.
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Pavuková, S.:Vinca minor L. alkaloids and their biological activity II. Diploma thesis, Charles University, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany, Hradec Králové 2020. Vinca minor L. is a species of species of flowering plant, native mainly to central and southern Europe, which containst more than 50 indole alkaloids. During screening of potential plant inhibitors against human acetylcholinesterase (hAChE) and butyrylcholinesterase (HBChE) at our department, an alkaloidal extract from dried aerial parts of Vinca minor demonstrated strong and selective hBChE inhibitory activity with an IC50 value of 13.60 ± 0.83 μg/mL, however, against hAChE was inactive (IC50 value >100 μg/mL). The fraction VM 323 - 327 (4,72 g) was separated by column chromatography on silica gel again with stepwise elution by using chloroform and ethanol and overall 7 joined fractions were obtained.Subsequently, repeated preparative TLC on silica gel led to isolation of three compounds; the newly isolated substance SP-1, (-)-picrinine (SP-2) and deacetylakuammiline (SP-3). Their structures were elucidated with mass spectrometry (ESI), NMR and optical rotation. Isolated alkaloids were tested on ability to inhibit AChE, BuChE, POP a GSK-3β, which are enzymes playing an important role in...