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Screening
Richter, Lucie ; Šafratová, Marcela (advisor) ; Cahlíková, Lucie (referee)
IX. ABSTRACT Charles University in Prague, Faculty of Pharmacy in Hradec Králové Department of: Pharmacognosy and Pharmaceutical Botany Candidate: MUDr. et Mgr. Lucie Richter Consultant: PharmDr. Marcela Šafratová, Ph.D. Title of Thesis: SCREENING STUDY OF SEVERAL PLANT SPECIES AND THEIR EFFECT ON HUMAN ENZYMATIC SYSTEMSII. Five tropical plants (Geissospermum vellosii stembark, Calotropis gigantea aerial part, Cissampelos pareira stem, Virola sebifera stembark and Virola surinamensis stembark) were screened for alkaloid presence and a preliminary estimate of their potential as anticholinesterase or cytotoxic agent was performed. Ethanolic extracts were prepared from these plants and further processed into the ethyl acetate alkaloid extracts, which were then analysed using the GC/MS method. For extracts with the confirmed presence of alkaloids (Geissospermum vellosii, Calotropis gigantea and Virola sebifera) by TLC including UV detection and Dragendorff test, the anticholinesterase activity against human AChE and BuChE was measured employing Ellman method and compared to standards (galantamine, huperzine A and rivastigmine). Cytotoxic activity of these extracts was also evaluated on Jurkat, MOLT-4, A549, HT-29, PANC-1, A2780, HeLa, MCF-7, SAOS-2 tumour cell lines and MRC-5 control cell line using MTT method...
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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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Secondary metabolites of familly Apocynaceae as a souce of cytotoxic substances
Měšťanová, Kristýna ; Šafratová, Marcela (advisor) ; Hradiská Breiterová, Kateřina (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacognosy and Pharmaceutical Botany Student: Kristýna Měšťanová Thesis supervisor: PharmDr. Marcela Šafratová, Ph.D. Thesis title: Secondary metabolites of the Apocynaceae family as a source of cytotoxically active substances The diploma thesis is focused on elaborating a comprehensive overview of secondary metabolites of the Apocynaceae family with a focus on their application in practice and the importance of Vinca alkaloids in the treatment of Hodgkin's and non- Hodgkin's disease. First, the major representatives of the Apocynaceae family, their constituents and mechanisms of action are mentioned. The uses and the desired and side effects are described and the effects of cardenolides are also stated. The work also deals with Hodgkin's and non-Hodgkin's disease, their incidence, symptomatology and classification of these diseases. Risk factors, including biological and genetic characteristics, are listed. Furthermore, the topic of staging and the treatment of these diseases according to the individual stages of the disease and differences in therapy of specific groups of patients are elaborated. The individual types of lymphomas, their diagnosis and subsequent treatment, including side effects, are described in detail. The...
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Indole alkaloids and their biological aktivity: genus Banisteriopsis
Nieslaniková, Karolina ; Šafratová, Marcela (advisor) ; Jenčo, Jaroslav (referee)
Author: Karolina Nieslaniková Name: Indole alkaloids and their biological activity: genus Banisteriopsis Diploma thesis Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of Pharmacognosy and Pharmaceutical Botany 2022, 69 p. Key words: Banisteriopsis, monoamine oxidase inhibitors (MAOi), Parkinson's disease, antidepressant activity, β- carbolines, harmine The aim of this research diploma thesis was to summarize all known information about indole alkaloids isolated from plants of the genus Banisteriopsis. Phytochemically important species of the genus Banisteriopsis were processed with an overview of botanical and phytochemical characteristics. Also in this thesis you can find an overview of alkaloids isolated from these plants and description of their biological activities. 10 plant species of the genus Banisteriopsis were processed phytochemically and botanically and there where identified a total of 14 alkaloids and 2 alkaloid glycosides. These alkaloids are divided into two groups: β-carbolines and tryptamines. The most important group of alkaloids in the genus Banisteriopsis consists of harmala alkaloids with neuroprotective, antidepressant, antitumor, antiadictive, anti-inflammatory, antimicrobial, antioxidant, antiplatelet and antidiabetic activity. Their...
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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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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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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 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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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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