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Alkaloids screening with a focus on potential drug discovery
Adamičková, Leona ; Opletal, Lubomír (advisor) ; Hošťálková, Anna (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Botany Candidate: Mgr. Leona Adamičková Supervisor: Prof. RNDr. Lubomír Opletal, CSc. Title of Rigorous Thesis: Alkaloids screening with a focus on potential drug discovery Key words: cholinesterase inhibition, Alzheimer disease, plant extract Within new anti-Alzheimer agent searching a screening of inhibition activity of various plants was performed. For this study plants used in traditional medicine were chosen and alkaloidal extracts were prepared and their potential to human cholinesterases inhibition was determined. For extraction bulbs of Fritillaria ussurensis, bulbs of F. cirrhosis, cortex and flowers of Magnolia officinalis, flowers of M. biondii, Nelumbo nucifera seeds, leaves and roots with rhizomes of Nuphar luteum, Papaver rheum roots, Laurus nobilis fruits and seeds of Ziziphus jujuba var. spinosa were used. The cholinesterase inhibitory activity was determined in vitro by modified Ellman's method. Extract of Fritillaria ussurensis bulbs was found to be the most potent inhibitor of BuChE with IC50 value of 11,63 ± 3,7 μg/mL. Extract of M. biondii inhibited both cholinesteras with IC50 values lower than 50 μg/mL. Among extracts with inhibition activity to BuChE pertain extracts of F. cirrhosa bulbs,...
Biological activity of plants secondary metabolites XXX. Basic search of selected taxons on anticholinesterase activity.
Karaščáková, Diana ; Opletal, Lubomír (advisor) ; Hošťálková, Anna (referee)
CHARLES UNIVERSITY Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Botany Candidate: Diana Karaščáková Supervisor: prof. RNDr. Lubomír Opletal, CSc. Title of diploma thesis: Biological activity of plants secondary metabolites XXX.; Basic search of selected taxons on anticholinesterase activity As part of the study of the biological activity of secondary metabolites, 7 taxa of higher plants were selected. The study deals with basic research of summary and alkaloid extracts prepared from morphological parts of plants Annona muricata (leaves), Leonotis leonurus (perch), Turnera diffusa (perch), Hamelia patens (perch), Uncaria guianensis (bark), Allamanda cathartica (perch) and Morinda citrifolia (leaves). To elucidate the presence of the major types of secondary metabolites, extracts were prepared and subjected to detection reactions by TLC using ten detection reagents. After detection by Dragendorff's reagent of ethyl acetate extracts, alkaloids were significantly present only in Annona muricata. Alkaloids were not detected in the bark of Uncaria guianensis. Using the Ellman method, the extracts were tested for potential inhibitory activity against human brain cholinesterases, using both recombinant enzymes. No significant active substances were present in any of the measured...
Natural substances and their biological activity.Screening of alkaloid plants for anticholinesterase effect
Valentová, Ivana ; Opletal, Lubomír (advisor) ; Hošťálková, Anna (referee)
1 ABSTRACT Charles University, Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Botany Candidate: Mgr Ivana Valentová Supervisor: Prof. RNDr. Lubomír Opletal, CSc. Title of Rigorous Thesis: Natural substances and their biological activity. Screening of alkaloid plants on human cholinesterases inhibition Key words: cholinesterase inhibition, Alzheimer disease, plant extract Ten herbs were screened for cholinesterase inhibition activity within searching new anti-Alzheimer agent. These plants are traditionally used as rerbal remedies for various diseases and they could be sources of new potential natural compounds. For this reason, ethanolic and alkaloidal extracts plants were prepared and their ability to inhibit human cholinesterases inhibition was determined. For the extraction Papaver somniferum immature capsules, Euonymus europeus fruits, Papaver orientale leaves, Magnolia officinalis leaves, Lycopodium clavatum aerial parts, Laurus nobilis leaves, Fritillaria imperialis bulbs, Flueggea suffruticosa aerial parts, Uncaria tomentosa bark, and Evolvulus alsinoides aerial parts were chosen. For the determination of human cholinesterase inhibitory activity in vitro modified Ellman's method was used. Only two alkaloidal plant extracts could be considered as potential source of HuBuChE...
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...
Biological aktivity of secondary plants metabolites X. Alkaloids of Vinca minor L.
Šípková, Pavla ; Hošťálková, Anna (advisor) ; Chlebek, Jakub (referee)
Šípková, P.: Biological activity of secondary plants metabolites X. Alkaloids of Vinca minor L. Diploma thesis, Charles University, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany, Hradec Králové, 2019, 66 s. Key words: Apocynaceae, Vinca minor, alkaloids, isolation, biological activity, screening Alzheimer's disease is a progressive neurodegenerative disease. The number of affected patients is constantly increasing. This disease cannot be treated casually, therefore discovering and testing new substances that could potentially be used in a treatment is very important. The Vinca minor L. fraction after column chromatography was separated by flash chromatography. Isolation of the individual alkaloids was performed by preparative TLC. Based on NMR and MS analyses and comparison with literature, alkaloids were identified as vincarubine and (-)-vinoxine. Modified Ellman's method was used to test cholinesterase inhibitory activity of isolated alkaloids. Acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) are enzymes, that play a very important role in the pathofysiology of Alzheimer's diasease. (-)-Vinoxine showed relatively high activity against BuChE (IC50 = 24,61 ± 1,71 µM), inhibitory activity against AChE was insignificant (IC50 > 1000µM). Vincarubin did not...
Biological activity of plants secondary metabolites XXX. Basic search of selected taxons on anticholinesterase activity.
Karaščáková, Diana ; Opletal, Lubomír (advisor) ; Hošťálková, Anna (referee)
CHARLES UNIVERSITY Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Botany Candidate: Diana Karaščáková Supervisor: prof. RNDr. Lubomír Opletal, CSc. Title of diploma thesis: Biological activity of plants secondary metabolites XXX.; Basic search of selected taxons on anticholinesterase activity As part of the study of the biological activity of secondary metabolites, 7 taxa of higher plants were selected. The study deals with basic research of summary and alkaloid extracts prepared from morphological parts of plants Annona muricata (leaves), Leonotis leonurus (perch), Turnera diffusa (perch), Hamelia patens (perch), Uncaria guianensis (bark), Allamanda cathartica (perch) and Morinda citrifolia (leaves). To elucidate the presence of the major types of secondary metabolites, extracts were prepared and subjected to detection reactions by TLC using ten detection reagents. After detection by Dragendorff's reagent of ethyl acetate extracts, alkaloids were significantly present only in Annona muricata. Alkaloids were not detected in the bark of Uncaria guianensis. Using the Ellman method, the extracts were tested for potential inhibitory activity against human brain cholinesterases, using both recombinant enzymes. No significant active substances were present in any of the measured...
Vinca minor L. alkaloids and their biological activity (inhibition of human cholinesterases) V.
Vašíčková, Alžběta ; Chlebek, Jakub (advisor) ; Hošťálková, Anna (referee)
Vašíčková A.: Alkaloids of Vinca minor L. and their biological activity (inhibition of human cholinesterases) V. Diploma thesis, Charles University, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany, Hradec Králové 2020. From the selected fraction VM 215-258 were isolated 3 alkaloids by flash chromatography followed, preparative thin layer chromatography and crystallization. Their structure was determined by mass spectroscopy, NMR and optical rotation, and the obtained data were compared with those in literature. Strictamine and minovincinine belong to alkaloids previously isolated, the alkaloid AV-3 has not been isolated yet. These alkaloids were tested for their ability to inhibit human cholinesterases and their inhibitory activity was compared to standards galanthamine and physostigmine. Compound AV-3 showed mild inhibitory activity against BChE (IC50 μM > 86.3 ± 2.3), other alkaloids were considered inactive, their IC50 values against cholinesterases were > 100 μM. Key words: Vinca minor L. (Apocynaceae), vinca alkaloids, minovincinine, strictamine, Alzheimer's disease, acetylcholinesterase, butyrylcholinesterase.
Nutraceuticals: possibilities in decreasing of hyperuricemia and alleviating gout
Lorencová, Štěpánka ; Hošťálková, Anna (advisor) ; Opletal, Lubomír (referee)
1 ABSTRACT Lorencová Š.: Nutraceuticals: possibilities in decreasing of hyperuricemia and alleviating gout. Diploma thesis, Charles University in Prague, Faculty of Pharmacy in Hradec Kralove, Department of Pharmaceutical Botany and Ecology, Hradec Kralove 2020, 82 p. This research work was conducted on the basis of literature analysis, reviewing papers mainly from international but also domestic journals. The review describes pathophysiology of gout and discusses options to mitigate the disease with the aid of dietary supplements. This work presents symptoms and a clinical picture of the disease as well as its origin and risk factors, pathological processes leading to the development of the disease, and a short overview of current pharmacotherapy. Furthermore this work summarises natural substances including plant extracts that may be utilised in the prevention and support of gout treatment. In particular, these include vitamins, unsaturated fatty acids, polyphenols and peptides. This work also describes plants used in the traditional treatment of gout and gives a brief overview of natural substances including plant extracts contained in food supplements that are available on the market in Czech Republic. This work also describes the role of purines, fructose, alcoholic drinks and tomatoes in triggering...
Biological aktivity of secondary plants metabolites X. Alkaloids of Vinca minor L.
Šípková, Pavla ; Hošťálková, Anna (advisor) ; Chlebek, Jakub (referee)
Šípková, P.: Biological activity of secondary plants metabolites X. Alkaloids of Vinca minor L. Diploma thesis, Charles University, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany, Hradec Králové, 2019, 66 s. Key words: Apocynaceae, Vinca minor, alkaloids, isolation, biological activity, screening Alzheimer's disease is a progressive neurodegenerative disease. The number of affected patients is constantly increasing. This disease cannot be treated casually, therefore discovering and testing new substances that could potentially be used in a treatment is very important. The Vinca minor L. fraction after column chromatography was separated by flash chromatography. Isolation of the individual alkaloids was performed by preparative TLC. Based on NMR and MS analyses and comparison with literature, alkaloids were identified as vincarubine and (-)-vinoxine. Modified Ellman's method was used to test cholinesterase inhibitory activity of isolated alkaloids. Acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) are enzymes, that play a very important role in the pathofysiology of Alzheimer's diasease. (-)-Vinoxine showed relatively high activity against BuChE (IC50 = 24,61 ± 1,71 µM), inhibitory activity against AChE was insignificant (IC50 > 1000µM). Vincarubin did not...
Bioactive metabolites of representative members in the genus Magnolia
Lakatošová, Ivana ; Hošťálková, Anna (advisor) ; Opletal, Lubomír (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Botany Candidate: Ivana Lakatošová Supervisor: PharmDr. Anna Hošťálková, Ph.D. Title of Master's thesis: Bioactive metabolites of representative members in the genus Magnolia 2019, 72 p. Key words: Magnolia, secondary metabolites, traditional medicine, CNS bioactivity The aim of this Master's thesis was to summarise current knowledge of significant secondary metabolites of species Magnolia officinalis and Magnolia obovata, and their biological activity. Botanical features of genus Magnolia were defined and described, followed by the classification of bioactive compounds isolated from species Magnolia officinalis and Magnolia obovata. The Master's thesis focused predominantly on the effects of biphenol compounds of magnolol and honokiol, which have been subjected to many studies. The main attention was given to the immunosuppressive effect and pharmacologic effects on the nervous system. Essential oils were observed to have an anti-inflammatory and a myorelaxant effect. Alkaloids and neolignans, which had been known to relax spasms of skeletal muscles, expressed neuroprotective activity. Neolignans were shown to have the inhibitory effect on bacteria, viruses and pathogenic fungi. They also proved themselves to be...

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