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Alkaloids of the family Amaryllidaceae and their biological aktivity I.
Puskásová, Dominika ; Šafratová, Marcela (advisor) ; Chlebek, Jakub (referee)
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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Cytotoxic and cholinesterase inhibitory activity of extracts from selected species of the Centaurea L. genus
Faschingbauer, Jakub ; Chlebek, Jakub (advisor) ; Šafratová, Marcela (referee)
Faschingbauer J.: Cytotoxic and cholinesterase inhibitory activity of extracts from selected species of the Centaurea L. genus. Diploma thesis, Charles University, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany, Hradec Králové, 2019. During the screening of biologically active secondary metabolites of plants carried out at the Department of Pharmaceutical Botany FAF UK, selected taxa of the genus Centaurea (Asteraceae) were investigated. This study is focused on a basic phytohemical research of extracts prepared from Centaurea cyanus, Centaurea jacea, Centaurea scabiosa, Centaurea pseudophrygia, Centuarea stoebe, Centaurea solstitialis a Centaurea benedicta. Extracts were prepared for evidence of the proof reactions of TLC and MS analysis (EI, ESI) to clarify a potential presence of alkaloids. EtOAc and ethanol extracts were evaluated for potential inhibitory activity against human erythrocyte acetylcholinesterase (AChE) and plasma butyrylcholinesterase (BChE) and cytotoxicity against selected 9 tumor lines. C. cyanus alkaloid extract had interesting cholinesterase activity which selectively inhibited BChE (IC50 BChE = 22.62 ± 3.62 μg / ml, IC50 AChE = 221.50 ± 44.56 g / ml). Other EtOAc extracts of selected Centaurea species were considered inactive (IC50 > 100 μg/ml)....
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Alkaloids of family Amaryllidaceae: genus Hippeastrum
Öhlschlegelová, Jana ; Hošťálková, Anna (advisor) ; Šafratová, Marcela (referee)
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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Alkaloids of the family Amaryllidaceae and their biological aktivity I.
Puskásová, Dominika ; Šafratová, Marcela (advisor) ; Chlebek, Jakub (referee)
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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Alkaloids of Narcissus pseudonarcissus cv. Dutch Master: isolation, structural identification, preparation of analogues, biological activity.
Schickerová, Julie ; Cahlíková, Lucie (advisor) ; Šafratová, Marcela (referee)
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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Alkaloids of Narcissus pseudonarcissus cv. Dutch Master: isolation, structural identification, preparation of analogues, biological activity.
Schickerová, Julie ; Cahlíková, Lucie (advisor) ; Šafratová, Marcela (referee)
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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Screening of various plant taxa and their influence on human enzyme systems I.
Šikola, Václav ; Šafratová, Marcela (advisor) ; Siatka, Tomáš (referee)
Šikola V.: Screening of various plant taxa and their influence on human enzyme systems I. Diploma thesis, Charles University, Faculty of Pharmacy in Hradec Králové, Department of Pharmacognosy, Hradec Králové 2018, 52 pages. The object of this diploma thesis was the screening of 5 chosen plant taxa (Desmodium adscendens, Codonopsis pilosula, Centella asiatica, Bacopa monnieri, Epimedium sagittatum) to identify chemical constituents (alkaloids) and to define inhibitory activity against human acetylcholinesterase (HuAChE) and butyrylcholinesterase (HuBuChE). Summary extract of plants was prepared by extraction to ethanol, the presence of alkaloids was verified by control TLC (UV, Dragendorff's reagent). Alkaloidal extracts were prepared by extraction of an alkaline solution of summary extracts to ethyl acetate. Alkaloidal extracts were subjected to GC/MS analysis and tested for their inhibitiory activity on human cholinesterases by Ellman's method. Results of GS/MS analysis did not provide information on contained alkaloids - the alkaloids did not gasify or were not contented. Conclusions of measuring inhibition activity of extracts in comparison to standards (galantamine, huperzine A) eliminated an usage of alkaloids in a clinical praxis because the activity was many times lower than standards. The...
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Alkaloids of family Amaryllidaceae: genus Zephyranthes
Jánská, Lucie ; Šafratová, Marcela (advisor) ; Hošťálková, Anna (referee)
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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Study of inhibition (toxicity) activity of alkaloids from selected plant species of Amaryllidaceae family on human enzyme systems (in vitro study) III
Šafratová, Marcela ; Cahlíková, Lucie (advisor) ; Kokoška, Ladislav (referee) ; Drašar, Pavel (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Botany and Ecology Candidate: Mgr. Marcela Šafratová Supervisor: Doc. Ing. Lucie Cahlíková PhD. Title of Doctoral Thesis: Study of inhibition (toxicity) activity of alkaloids from selected plant species of Amaryllidaceae family on human enzyme systems (in vitro study) III Key words: Narcissus poeticus cv. Pink Parasol, Amaryllidaceae, alkaloids, acetylcholinesterase, butyrylcholinesterase, prolyl oligopeptidase, cytotoxicity Bulbs of Narcissus poeticus. cv. Pink Parasol were selected as a source of Amaryllidaceae alkaloids for study of their biological activity. Concentrated alkaloid extract has been prepared were prepared by standard extraction and fractionated in aluminium oxide column chromatography column using step gradient elution with petrol, chloroform and ethanol. Column chromatography, vacuum liquid column chromatography, preparative TLC and crystallizations resulted in the isolation of 15 alkaloids, 2 of them were identified as new structures. The chemical structures of isolated compounds were determined on the basis of spectrometric techniques (NMR, MS, optical rotation) and by comparison with literature. Alkaloids isolated in sufficient amounts were tested on their inhibitory ability of human...
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Study of inhibition (toxicity) activity of alkaloids from selected plant species of Amaryllidaceae family on human enzyme systems (in vitro study) III
Šafratová, Marcela ; Cahlíková, Lucie (advisor) ; Drašar, Pavel (referee) ; Kokoška, Ladislav (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Botany and Ecology Candidate: Mgr. Marcela Šafratová Supervisor: Doc. Ing. Lucie Cahlíková PhD. Title of Doctoral Thesis: Study of inhibition (toxicity) activity of alkaloids from selected plant species of Amaryllidaceae family on human enzyme systems (in vitro study) III Key words: Narcissus poeticus cv. Pink Parasol, Amaryllidaceae, alkaloids, acetylcholinesterase, butyrylcholinesterase, prolyl oligopeptidase, cytotoxicity Bulbs of Narcissus poeticus. cv. Pink Parasol were selected as a source of Amaryllidaceae alkaloids for study of their biological activity. Concentrated alkaloid extract has been prepared were prepared by standard extraction and fractionated in aluminium oxide column chromatography column using step gradient elution with petrol, chloroform and ethanol. Column chromatography, vacuum liquid column chromatography, preparative TLC and crystallizations resulted in the isolation of 15 alkaloids, 2 of them were identified as new structures. The chemical structures of isolated compounds were determined on the basis of spectrometric techniques (NMR, MS, optical rotation) and by comparison with literature. Alkaloids isolated in sufficient amounts were tested on their inhibitory ability of human...
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