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Alkaloids from Vinca minor L. and their biological activity.
Vrabec, Rudolf ; Opletal, Lubomír (advisor) ; Kokoška, Ladislav (referee) ; Lapčík, Oldřich (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Pharmacognosy and Pharmaceutical Botany Candidate: Mgr. Rudolf Vrabec Supervisor: prof. RNDr. Lubomír Opletal, CSc. Title of doctoral thesis: Alkaloids from Vinca minor L. and their biological activity Key words: Vinca, indole alkaloids, Alzheimer's disease, AChE, BuChE, POP, GSK-3β, cytotoxicity, docking study Twenty-three monoterpene indole alkaloids of different structural types were isolated by chromatographic techniques from aerial parts of Vinca minor L. (Apocynaceae). The alkaloids were identified by a combination of analytical methods (NMR, MS, HRMS, optical rotation). Among obtained compounds, one structure was undescribed so far and was named vincaminorudeine. Eleven alkaloids were isolated for the first time from this species. Obtained compounds that were isolated in sufficient amounts were subjected to in vitro tests for the inhibition of hAChE, hBuChE, POP, and GSK-3β - enzymes that play a key role in the pathophysiology of Alzheimer's disease. The most active alkaloid was (−)-2-ethyl-3[2-(3-ethylpiperidinyl)-ethyl]-1H- indole (VR-19) with IC50 = 0,65 µM for the inhibition of hBuChE, and with IC50 = 58 µM for the inhibition of POP. Other alkaloids which exhibited a significant inhibition against hBuChE (IC50 30...
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Alkaloids from Vinca minor L. and their biological activity.
Vrabec, Rudolf ; Opletal, Lubomír (advisor) ; Kokoška, Ladislav (referee) ; Lapčík, Oldřich (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Pharmacognosy and Pharmaceutical Botany Candidate: Mgr. Rudolf Vrabec Supervisor: prof. RNDr. Lubomír Opletal, CSc. Title of doctoral thesis: Alkaloids from Vinca minor L. and their biological activity Key words: Vinca, indole alkaloids, Alzheimer's disease, AChE, BuChE, POP, GSK-3β, cytotoxicity, docking study Twenty-three monoterpene indole alkaloids of different structural types were isolated by chromatographic techniques from aerial parts of Vinca minor L. (Apocynaceae). The alkaloids were identified by a combination of analytical methods (NMR, MS, HRMS, optical rotation). Among obtained compounds, one structure was undescribed so far and was named vincaminorudeine. Eleven alkaloids were isolated for the first time from this species. Obtained compounds that were isolated in sufficient amounts were subjected to in vitro tests for the inhibition of hAChE, hBuChE, POP, and GSK-3β - enzymes that play a key role in the pathophysiology of Alzheimer's disease. The most active alkaloid was (−)-2-ethyl-3[2-(3-ethylpiperidinyl)-ethyl]-1H- indole (VR-19) with IC50 = 0,65 µM for the inhibition of hBuChE, and with IC50 = 58 µM for the inhibition of POP. Other alkaloids which exhibited a significant inhibition against hBuChE (IC50 30...
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Alkaloids from Selected Species of Amaryllidaceaefamily, their Toxicity and Biological Activity (in vitro study) I.
Krejčí, Andrea ; Cahlíková, Lucie (advisor) ; Grančai, Daniel (referee) ; Kokoška, Ladislav (referee)
Charles University in Prague, Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Botany and Ecology Candidate Mgr. Andrea Krejčí, née Kulhánková Supervisor Ing. Lucie Cahlíková, Ph.D. Title of Doctoral Thesis Alkaloids from selected species of Amaryllidaceae family, their toxicity and biological activity (in vitro study) I. Zephyranthes robusta and Chlidanthus fragrans bulbs were chosen for phytochemical study as biologically active Amaryllidaceae alkaloids source, based on bio-guided study using spectrophotometric Ellman's method and GC-MS analysis of alkaloid extracts. Bulbs were extracted with ethanol and the summary extract was fractionated by column chromatography with the use of Al2O3 as a stationary phase and gradient elution chloroform - ethanol. Column chromatography, preparative TLC and crystallisation led to isolation of pure compounds the chemical structure of which was elucidated by MS and D1- and D2-NMR analyses. From fresh bulbs of Chlidanthus fragrans 11 alkaloids were isolated of which deoxypretazzetine, belladine, 3-epimakronine, ismine, undulatine, buphanisine and ambelline were reported for the first time from the genus Chlidanthus. Compounds were evaluated for their human AChE, BuChE and POP inhibitory activity. From Zephyranthes robusta bulbs 14 alkaloids of...
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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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Study of Chemical Constituents of Taxons from Order Laurales and Ranunculales with Potential Neuroprotective Activity
Hošťálková, Anna ; Opletal, Lubomír (advisor) ; Kokoška, Ladislav (referee) ; Drašar, Pavel (referee)
Charles University in Prague, Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Botany and Ecology Candidate: Mgr. Anna Hošťálková Supervisor: Prof. RNDr. Lubomír Opletal, CSc. Title of Doctoral Thesis: Study of chemical constituents of taxons from order Laurales and Ranunculales with potential neuroprotective activity. Key words: Berberis vulgaris, Peumus boldus, Hydrastis canadensis, isoquinoline alkaloids, acetylcholinesterase, butyrylcholinesterase, prolyl oligopeptidase. Commercial goldenseal extrakt, boldo leaves and barberry root bark were selected as sources of isoquinoline alkaloids for study of their biological activity. Mixtures of summary tertiary alkaloids were prepared by standard extraction and subsequently fractionated in aluminium oxide chromatography column using the step gradient elution with petrol, chloroform and ethanol. Repeated column chromatographies, preparative TLC and crystallizations led to the isolation of 28 isoquinoline alkaloids, 6 of them were identificated as new structures (some of them were propably artifacts). The chemical structures of isolated compounds were determined on the basis of spectrometric techniques (NMR, MS) and by comparison with literature. Isolated alkaloids in sufficient amount were tested on ability to inhibit human...
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Aspects of the use of herbal preparations adult population in the Czech Republic
Knotek, Karel ; Kokoška, Ladislav (advisor) ; Zelený, Václav (referee) ; Jahodář, Luděk (referee)
The subject of this thesis is to map the approach and behaviour of the adult population in the Czech Republic as regards the use of plant products (PP), both medicinal plants and herbal dietary supplements. For the public, the high prevalence of PP is a good opportunity to use such plants for self-medication or to prevent illness. The general part of this thesis describes the characteristics and importance of both groups of plant products, as well as the topical issue of the choice, use and role of these plants in the world and in the Czech Republic on the basis of research. The practical part then presents the results of a questionnaire survey of people who use plant products - customers of pharmacies in selected regions of the Czech Republic: the capital, Prague, the Region of North Bohemia, and the Region of South Bohemia. Based on classification attributes the work monitors the public's approach and behaviour as regards the choice and means of acquiring and using PP and activity in relation to self-medication, such as consulting the suitable selection of PP or people informing their doctor that they are using PP. The work ascertains to what extent users know about and are aware of medicinal plants, how they are collected and used, and their properties on which the respondents base their choice...
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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 Chemical Constituents of Taxons from Order Laurales and Ranunculales with Potential Neuroprotective Activity
Hošťálková, Anna ; Opletal, Lubomír (advisor) ; Kokoška, Ladislav (referee) ; Drašar, Pavel (referee)
Charles University in Prague, Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Botany and Ecology Candidate: Mgr. Anna Hošťálková Supervisor: Prof. RNDr. Lubomír Opletal, CSc. Title of Doctoral Thesis: Study of chemical constituents of taxons from order Laurales and Ranunculales with potential neuroprotective activity. Key words: Berberis vulgaris, Peumus boldus, Hydrastis canadensis, isoquinoline alkaloids, acetylcholinesterase, butyrylcholinesterase, prolyl oligopeptidase. Commercial goldenseal extrakt, boldo leaves and barberry root bark were selected as sources of isoquinoline alkaloids for study of their biological activity. Mixtures of summary tertiary alkaloids were prepared by standard extraction and subsequently fractionated in aluminium oxide chromatography column using the step gradient elution with petrol, chloroform and ethanol. Repeated column chromatographies, preparative TLC and crystallizations led to the isolation of 28 isoquinoline alkaloids, 6 of them were identificated as new structures (some of them were propably artifacts). The chemical structures of isolated compounds were determined on the basis of spectrometric techniques (NMR, MS) and by comparison with literature. Isolated alkaloids in sufficient amount were tested on ability to inhibit 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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