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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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Biologically active metabolites of plants. 10. Alkaloids of Fumaria officinalis L. and their biological activity
Šafratová, Marcela ; Cahlíková, Lucie (advisor) ; Jahodář, Luděk (referee)
Šafratová M.: Biologically active metabolites of plants 10. Alkaloids of Fumaria officinalis L. and their biological aktivity. Charles University in Prague, Faculty of Pharmacy in Hradec Králové. Department of Pharmaceutical Botany and Ecology, Hradec Králové, 2013. Diploma thesis. 70 s. The object of this diploma thesis was to process the pool of alkaloids from Fumaria officinalis L. (Fumariaceae). Using column chromatography and preparative TLC three alkaloids were isolated which have been subjected to structural analysis (MS, NMR). The first substance was identified as isoquinoline alkaloid stylopin, others isolated alkaloid was sinactin and third isolated alkaloid was fumarilin. All three alkaloids have been previously isolated from F. officinalis. For all three alkaloids were tested for their inhibitory activity against human erythrocyte acetylcholinesterase (HuAChE) and human serum butyrylcholinesterase (HuBuChE). For stylopine IC50 values were determined IC50 HuAChE ˂ 1000 µM and IC50 HuBuChE ˂ 1000 µM. For sinactine were measured IC50 HuAChE = 632 ± 22 µM and IC50 HuBuChE ˂ 1000 µM. Values for fumariline IC50 HuAChE ˂ 1000 µM and IC50 HuBuChE = 330 ± 12 µM. In comparison with standards were stylopine, sinactine and fumariline not very active. None of the isolated compounds are therefore...
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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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Isolation of alkaloids of the species Geissospermum vellosii Allemão and study of their biological activity I.
Buláková, Anna ; Šafratová, Marcela (advisor) ; Siatka, Tomáš (referee)
Buláková, A: Isolation of alkaloids of the species Geissospermum vellosii Allemão and study of their biological activity I. Diploma thesis, Charles University, Faculty of Pharmacy in Hradec Králové, Department of Pharmacognosy, Hradec Králové, 2020. Key words: Geissospermum vellosii, bark, alkaloidal extracts, isolation of alkaloids, GC/MS analysis, biological activity, acetylcholinesterase, butyrylcholinesterase. Geissospermum vellosii as a plant belongs to the Apocynaceae family, whose bark is characterized by the content of indole alkaloids, which can also act as acetylcholinesterase inhibitors. The aim of this thesis was to process the pool of ethereal and chloroformic alcaloids from the plant Geissospermum vellosii. By means of column chromatography, the ethereal pool was processed into subfractions GV-1 to GV-16. Taking advantage of preparational method TLC, the subfraction GV-11 was processed, of which one alcaloid-based substance was isolated. Its structure was determined based on GC-MS and NMR analysis and after comparing obtained data with the literature, the substance was identified as Normacusin B. The substance, we extracted, was of unstable nature and because of that, we could not research its biological activity further in relation to AChE and BuChE. Due to the instable nature of...
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Vinca minor L. alkaloids and their biological activity VIII.
Hojgrová, Veronika ; Chlebek, Jakub (advisor) ; Šafratová, Marcela (referee)
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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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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