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Screening of biological activity of various species of the genus Narcissus sp. I
Komendová, Karolína ; Suchánková, Daniela (advisor) ; Chlebek, Jakub (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Pharmacognosy and Pharmaceutical botany Candidate: Karolína Komendová Supervisor: PharmDr. Daniela Hulcová, Ph.D. Title of thesis: Screening of biological activity of various species of the genus Narcissus sp. I Key words: Amaryllidaceae, Narcissus, alkaloids, AChE, BuChE, Alzheimer's disease Alkaloids from family Amaryllidaceae (AA) nowadays belong to the most important and also the most examined alkaloids. This is because of their structural diversity and a broad spectrum of biological effects. The main aim of my diploma was to prepare whole bulb extracts from seven different cultivated varieties of genus Narcissus and to select those with the highest potential to inhibit enzyme acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). Inhibition of these enzymes is very important in the treatment of Alzheimer's disease (AD). Summary extracts were obtained from these cultivars: N. cv, Apotheose (AL - 718), N. cv. Chromacolor (AL - 722), N. cv. Hungarian Rhapsody (AL - 729), N. cv. Mon Cheri (AL - 736), N. cv. Peach Cobbler (AL - 738), N. cv. Pink Pride (AL - 740) a N. cv. Red Devon (AL - 742). The isolated extracts were subsequently analyzed by GC-MS. The following alkaloids were found in the majority of extracts:...
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Isolation of alkaloids from Hippeastrum ferrari and their biological activity
Buchalová, Tereza ; Suchánková, Daniela (advisor) ; Hradiská Breiterová, Kateřina (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Pharmacognosy and Pharmaceutical Botany Candidate: Tereza Buchalová Supervisor: PharmDr. Daniela Hulcová, Ph.D. Title of Thesis: Isolation of alkaloids from Hippeastrum cv. Ferrari and their biological activity Many different species, varieties, and cultivars of the genus Hippeastrum are popular indoor ornamental plants, but they also represent a rich source of important secondary metabolites called Amaryllidaceae alkaloids. These structurally unique compounds are known for their wide spectrum of biological activities such as anticancer, antiviral, and inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) which represent important part in therapy of Alzheimer's disease (AD). AD is a neurodegenerative disease that is identified as one of the most frequent causes of dementia in the world. Deficit of the neurotransmitter acetylcholine (ACh) in the cortex participates on the development of the AD, which results in the damage of cholinergic functions, and this is responsible for the memory loss and behavioural changes. AChE and BChE are enzymesinvolved in the termination of impulse transmission by rapid hydrolysis of ACh. Therefore, AChE and BChE inhibitors are nowadays the most important goal in...
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Isolation of alkaloids of the species Geissospermum vellosii Allemão and study of their biological activity VI.
Váňová, Lucie ; Šafratová, Marcela (advisor) ; Chlebek, Jakub (referee)
Lucie Váňová: Isolation of alkaloids of the species Geissospermum vellosii Allemão and study of their biological activity IV. Diploma thesis, Charles University, Faculty of Pharmacy in Hradec Králové, Department of Pharmacognosy and Pharmaceutical Botany, Hradec Králové 2022. Key words: bark, Geissospermum vellosii Allemão, alkaloids, preparative TLC, GC-MS, NMR, (+)-19,20-dehydrotubifolidine, aspidolimidine, geissoreticulatine, inhibition activity, AChE, BuChE, Alzheimer's disease The aim of this diploma thesis was the isolation of at least 3 alkaloids in pure form from the GV-5 fraction, which was extracted from the bark of the South American tree Geissospermum vellosii Allemão. By using preparative thin layer chromatography (TLC), 9 subfracions (GV-5-A až GV-5-I) were acquired from this fraction. Those that were of sufficient mass were subsequently subjected to further division. Three alkaloids in pure form were isolated through purification using preparative TLC: GV-5-B-3-A, GV-5-C-4-C, GV-5-C-2-B-1. Gained active substances from this plant were analyzed by gas chromatography- mass spektrometry (GC-MS) and nuclear magnetic resonance (NMR). By comparing the obtained alcaloid's spectra with available data and literature, those alkaloids were identified as: (+)-19,20-dehydrotubifolidine...
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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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