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Isolation of alkaloids of the species Geissospermum vellosii Allemão and study of their biological activity VIII.
Pelnář, Tomáš ; Šafratová, Marcela (advisor) ; Siatka, Tomáš (referee)
ISOLATION OF ALKALOIDS OF THE SPECIES GEISSOSPERMUM VELLOSII ALLEMÃO AND STUDY THEIR BIOLOGICAL ACTIVITY VIII. PELNÁŘ T. 1 , JANOUŠEK J. 2 , HRADISKÁ BREITEROVÁ K. 1 , ŠAFRATOVÁ M. 1 1 Department of Pharmacognosy and Pharmaceutical Botany, Faculty of Pharmacy in Hradec Králové, Charles University in Prague, Czech Republic 2 Biomedical Research Center, University Hospital in Hradec Králové, Czech Republic e-mail: pelnart@faf.cuni.cz The aim of this work was to determine the activity of indole alkaloids, including their separation and purification from the South American tree Geissopsermum vellossi, which is used in traditional medicine to treat various diseases. It shows possible use in the treatment of benign prostatic hyperplasia, tumor treatment, plasmodial diseases, and especially cognitive disorders. The isolated structures were subsequently tested for inhibition of human cholinesterases.1 These substances could be used to treat Alzheimer's disease, which has been increasing in recent years. We are not yet able to stop disease, just slow it down. The starting product was a summary alkaloid extract from crushed tree bark, which showed very interesting activity against AChE and BChE (IC50 = 15,19±0,96 µg/ml for AChE and IC50 = 0,37±0,049 µg/ml for BChE). The GV-4 fraction has been processed using...
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Biological activity of plant metabolites XXVIII. Alkaloids from selected cultivars of Narcissus cyclamineus REDOUTÉ and their influence on acetylcholinesterase and butyrylcholinesterase
Janura, Michal ; Opletal, Lubomír (advisor) ; Chlebek, Jakub (referee)
Biological activity of plant metabolites XXVIII. Alkaloids from selected cultivars of Narcissus cyclamineus REDOUTÉ and their influence on acetylcholinesterase and butyrylcholinesterase. JANURA M.: Diploma work, Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany and Ecology, Hradec Králové 2015, Czech Republic. Abstract: The summary extracts of alkaloids from bulbs of N. cyclamineus esp. N. cyclamineus cv. Jenny, N. cyclamineus cv. Little Witch, N. cyclamineus cv. Rapture, N. cyclamineus cv. Surfside, N. cyclamineus cv. Peeping Tom, N. cyclamineus cv. Warbeld and N. cyclamineus cv. Skater's Waltz were obtained by the procedures common for this type of compounds. The alkaloid extracts were analyzed by GC/MS and the probable occurrence of individual alkaloid substances was observed. These extracts were also assayed for HuAChE and HuBuChE inhibitory activity. N. cyclamineus cv. Surfside with IC50 = 61,26 ± 6,42 µg/ml and N. cyclamineus cv. Warbeld with IC50 = 85,43 ± 11,13 µg/ml have the best results in inhibition of HuBuChE. The best inhibitory activity on HuAChE has N. cyclamineus cv. Warbeld with IC50 (HuAChE) = 36,82 ± 4,50 µg/ml. Key words: Narcissus, Acetylcholinesterase, Butyrylcholinesterase, GC/MS, Alzheimer's disease.
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Alkaloids of the genus Narcissus and their biological aktivity
Tanková, Sabina ; Hulcová, Daniela (advisor) ; Opletal, Lubomír (referee)
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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Alkaloids of the genus Narcissus and their biological aktivity
Tanková, Sabina ; Hulcová, Daniela (advisor) ; Opletal, Lubomír (referee)
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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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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Biological activity of plant metabolites XXIX. Alkaloids from selected cultivars of Narcissus triandrus L. and their influence on acetylcholinesterase and butyrylcholinesterase
Farkašovský, Marek ; Opletal, Lubomír (advisor) ; Siatka, Tomáš (referee)
Farkašovský M.: Biological activity of plant metabolites XXIX. Alkaloids of selected cultivars of Narcissus triandrus L. and their influence on acetylcholinesterase and butyrylcholinesterase. Diploma thesis. Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of pharmaceutical botany and ecology, Hradec Králové 2015, 70 pages Screening of seven bulb samples of Narcissus genus was performed. It included cultivars Narcissus triandrus cv. Hawera, Narcissus triandrus cv. Ice Wings, Narcissus triandrus cv. Stint, Narcissus triandrus cv. Tresamble, Narcissus cyclamineus cv. February Gold, Narcissus cyclamineus cv. Greenlet and Narcissus cyclamineus cv. Itzim. Primary extract was prepared by boiling crushed bulbs in ethanol 95% and then it was condensated. After extraction in diethyl ether and ethyl acetate was pure alkaloid extract dried with air flow in water bath. Isolated alkaloid extracts were tested for their inhibition activity on acetylcholinesterase and butyrylcholinesterase. Also GC-MS analysis was provided to identify alkaloids. These alkaloids were identified with GC-MS analysis - epinorgalanthamine, galanthamine, galanthine, haemanthamine, hippeastrine, homolycorine, cherylline, incartine, lycoramine, lycoramine-acetate, lycorine, narwedine, neruscine, sanguinine...
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Alkaloids of the family Amaryllidaceae and their biological aktivity II.
Kosturko, Štefan ; Šafratová, Marcela (advisor) ; Cahlíková, Lucie (referee)
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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Isolation of alkaloids of the species Geissospermum vellosii Allemão and study of their biological activity IV.
Emrichová, Eliška ; Šafratová, Marcela (advisor) ; Hradiská Breiterová, Kateřina (referee)
Eliška Emrichová: Isolation of alkaloids of the species Geissospermum vellosii Allemão and study of their biological activity IV. Diploma thesis 2020. Charles University, faculty of Pharmacy in Hradec Králové, Department of Pharmacognosy. Key words: Geissospermum vellosii, bark, alkaloidal extracts, isolation of alkaloids, GC/MS analysis, biological aktivity, acetylcholinesterase, butyrylcholinesterase. The aim of this study was to isolate at least one pure alkaloid from the extract of Geissospermum vellosii Alemão bark. The whole process involved bark processing, to obtain summary and alkaloid extract and subsequent column chromatography. GV-4, one of the 16 obtained fractions, was separated into 5 subfractions. The GV-4bsubfraction was used to isolate pure alkaloids, processed by preparative thin layer chromatography and crystallization of pure compound. The structure of pure compound was determined by using NMR, GC-MS analysis and optical rotation. This compound was identified as anhydropereirine and was tested its inhibitory activity against human cholinesterases, AChE and BuChE. The alkaloids GV-1-a, GV-8-3-B, GV-9-c were isolated in the course of further work on the extract. Their inhibitory activity against GSK-3β was tested as well as their possibility to cross the blood-brain-barieer with...
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Alkaloids of the family Amaryllidaceae and their biological aktivity II.
Kosturko, Štefan ; Šafratová, Marcela (advisor) ; Cahlíková, Lucie (referee)
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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Isolation of alkaloids of the species Geissospermum vellosii Allemão and study of their biological activity III.
Růžička, Lukáš ; Šafratová, Marcela (advisor) ; Hulcová, Daniela (referee)
Růžička, L. Isolation of alkaloids from Geissospermum vellosii Allemão and study of their biological activity. Diploma thesis, Department of pharmacognosy, Faculty of Pharmacy in Hradec Králové, Charles University, Czech Republic, 2020. The aim of this diploma thesis are alkaloids from Geissospermum vellosii. This tree native in South America is commonly used for treatment of various diseases, including cognitive deficits in elder people1 . The study is based on previous research that was focused on inhibition of human cholinesterases and glycogensynthase 3 β(GSK-3 β), which can be used in treatment of Alzheimer disease. Incidence of this disease is rising up in the last decades and it represents a big burden for both health service and economy of developed countries2 . Isolation was carried out from crude crushed stembark. After extraction and agitation, 50.4 g of thick yellowish ether extract was obtained. This extract showed activity against cholinesterases (IC50 AChE = 15.19 ± 0.96 μg/ml and IC50 BuChE = 0.37 ± 0.049 μg/ml). Later, this extract was separated to 16 fractions by column chromatography. Fraction GV9 was chosen for additional research. Thin layer chromatography was carried out for purification and extraction of white crystalline alkaloid. Structure was determined by...
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