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Biological activity of macromycetes I.
Vyletelka, Juraj ; Macáková, Kateřina (advisor) ; Opletal, Lubomír (referee)
Vyletelka, Juraj. Biological activity of macromycetes I. Master Thesis 2012. Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany and Ecology. Supervisor: Ing. Kateřina Macáková, PhD. Key words: Ascomycota, Basidiomycota, acetylcholinesterase, butyrylcholinesterase, alkaloids, antioxidant activity, DPPH, ABTS, total phenolics. Macromycetes are the source of bioactive substances that still have not been completely researched. Many of them are used in treatment and they are the object of a growing interest. This work focuses on the measurement of biological activity of 25 ethanolic extracts prepared from various mushroom species. Ellman's spectrophotometric method was used to determine the acetylcholinesterase and butyrylcholinesterase inhibitory activities. The aim of the thin layer chromatography was to detect alkaloids. This work also deals with the determination of antioxidant activity by DPPH and ABTS+ radical scavenging assays modified for use with sequential injection analysis. The content of total phenolic compounds in extracts was determined using the Folin-Ciocaulteu method. Following the results of the presented methods, one may state that the extracts did not exhibit any significant inhibitory activity towards human cholinesterases....
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Biological activity of plants metabolites.XVII.Alkaloids of Corydalis yanhusuo W.T.WANG.
Cipra, Gabriella ; Opletal, Lubomír (advisor) ; Macáková, Kateřina (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Botany and Ecology Candidate: Gabriella Cipra Consultant: Assoc. Prof. RNDr. Lubomir Opletal, CSc. Title of Thesis: Biological activity of plant metabolites XVII. Alkaloids of Corydalis yanhusuo W.T. Wang In the process of screening for plants containing alkaloids potentially inhibiting human erythrocytic AChE and human BuChE, Corydalis yanhusuo was studied. 10.8 kg of dried tuber was percolated with 120 liters of 95% ethanol. From the primary extract, extracts with individual types of alkaloids were prepared. In this diploma thesis only one extract was processed (extract type A-ether, pH 9.7). Alkaloids from this extract were separated into bases which chlorides were either soluble or insoluble in chloroform. From each of the above mentioned fractions phenolic and non- phenolic alkaloids were obtained. Alkaloids were separated from extract of non-phenolic chlorides soluble in chloroform. From this mixture (+)-corydaline (labeled GC-1) was isolated by the use of column chromatography on alumina and preparative TLC on silica gel. This compound was preliminary identified according to data of MS spectra, NMR spectra, and optical rotation and by comparison with literature data. The biological activity of...
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Biological activity of plant metabolites I. Influence of plant constituents on some species of the genus Eimeria
Kvapilová, Jana ; Opletal, Lubomír (advisor) ; Tilšer, Ivan (referee)
SOUHRN K přípravě extraktů a následnému testování bylo na základě literatury vybráno několik drog - Caryophylli flos, Curcumae longae radix, Ocimi sancti herba, Origani herba a jedna izolovaná substance knicin (z Cardui benedicti herba). Z těchto drog jsem metodou kontinuální extrakce (perkolace) připravila extrakty a poté u nich stanovila sušinu. Potřebné množství zhomogenizovaného extraktu jsem sorbovala na celozrnnou mouku tak, aby v konečném množství roztěru 200 g byly nasorbovány 2 g suchého extraktu a byl dokonale homogenní. Tento roztěr byl dispergován do krmiva pro myši a krysy tak, aby výsledná koncentrace byla 100 ppm. V případě knicinu jsem obdržela již izolovanou substanci, příprava roztěru probíhala obdobným způsobem. Každý z extraktů a knicin byly testovány v jednom experimentu, jehož délka se pohybovala kolem asi 7 - 8 dnů. Testovaná látka byla podávána pokusné skupině zvířat (mastomyši a myši CD1) v krmivu, kontrolní skupina zvířat dostávala stejné krmivo, ale bez přídavku testované látky. Kokcidiostatický efekt se zjišťoval jako rozdíl v kvantitě vylučovaných oocyst mezi testovanou a kontrolní skupinou. Dle grafu 19 je patrné, že nejlepší kokcidiostatickou aktivitu vykazovaly tři extrakty připravené z drog Ocimi sancti herba, Caryophylli flos a Origani herba. U Ocimi sancti herba bylo...
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Use of kinase modulation in the Alzheimerʼs disease pathogenesis.
Polzerová, Iveta ; Chlebek, Jakub (advisor) ; Opletal, Lubomír (referee)
Polzerová, I: Use of kinase modulation in the Alzheimer's disease pathogenesis. Diploma thesis, Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany and Ecology, Hradec Králové 2016, 91 p. Data used in this Diploma Thesis have been taken from foreigner scientific literary sources. It provides the summary of the not yet explored natural compounds from marine organisms with kinase inhibitory activity. The first chapter Alzheimer's disease describes a characteristic of the disease, its etiopathogenesis, risk factors and currently available treatment. At the beginning of the second chapter are mentioned new perspective approaches to treatment of Alzheimer's disease. Most of this chapter deals with kinases as potential therapeutic targets in the treatment of Alzheimer's disease. In the chapter, physiologic and pathophysiologic functions of GSK-3β and CK-1δ are described in the organism, and also, other kinases are mentioned which are involved in the pathogenesis of the disease. Next part dedicates analytical methods suitable for testing activity and inhibition of kinases in vitro and in silico, also deals with summary of the synthetic kinase inhibitors and characterizes an their properties. In this chapter is also described main part of this work - the...
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Phytochemical study of Helianthus annuus L. II
Niedobová, Soňa ; Karlíčková, Jana (advisor) ; Opletal, Lubomír (referee)
OF THE DIPLOMA THESIS My diploma thesis was intended on phytochemical study of polar extract of Helianthus annuus L. leaves and simultaneously biological tests were done (so-called bioassay - guided separation) - acute toxicity, antioxidant activity (DPPH test, FRAP metod) and antifungal activity. The Fraction 29 showed the highest antioxidant activity. The Fraction 22-24/3, obtained by preparative chromatography, was analyzed by gas chromatography. This analysis shows present of the oil-acid, the oily acids with a middle chain, the palmitoic acid and the myristic acid.
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Biological activity of plant metabolites XI. Alkaloids of Corydalis cava (L.) Schweigg & Körte (Fumariaceae) and their influence on acetylcholinesterase
Sekula, Marek ; Opletal, Lubomír (advisor) ; Cahlíková, Lucie (referee)
Sekula, M.: Biological activity of plant metabolites XI.; Alkaloids of Corydalis cava (L.) Schweigg. & Körte (Fumariaceae) and their activity on acetylcholinesterase. Diploma thesis, Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany and Ecology, Hradec Králové 2009, 61 p. Within the screening of plants that contains alkaloids inhibiting the aktivity of the human erythtocytic acetylcholinesterase and human serum butyrylcholinesterase Turkey Corn (Corydalis cava (L.) Schweigg. & Körte, Fumariaceae) was studied. 11,3 kg of the dry roots served for the isolation of alkaloids. Extrakt "B-chloroform" wich contain mixture of terciary alkaloids bad diethylether-insoluble were obtained from the purified ethanolic extract. The task was to separate mixture of alkaloids from extrakt "B-chloroform". Using both column and thin layer chromatography sinoacutine as a base was isolated. The identity of the isolated alkaloid as determined by means of comparing its physico-chemical characteristics with the published data. The isolated sinoacutine inhibited the human erythrocytic acetylcholinesterase and human serum butyrylcholinesterase with IC50 for AChE (1,510 × 10-3 M) and with IC50 for BuChE (1,806 × 10-3 M). Comparing its biological aktivity with that of...
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Biologically active metabolites of plants. 2. Alkaloids from Chelidonium majus L. and their inhibiting activity to acetycholinesterase.
Novotná, Magdalena ; Cahlíková, Lucie (advisor) ; Opletal, Lubomír (referee)
Novotná M.: Biological Aktive Plant Metabolites 2. Alkaloids of Chelidonium majus L. and Their Inhibitory Activity against Acetylcholinesterase. Diploma thesis, Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany and Ecology, Hradec Králové 2010, 64 p. The aim of diploma thesis was to process of pool of alkaloids of Chelidonium majus, chlorids insoluble in chlorophorm for at least one alkaloid isolated in pure form and for the determination of anticholinesterase, antihelminth and antioxidant activity. Of the pool in this thesis were isolated by column chromatography two alkaloids. Based on NMR and MS study was the first substance MN-1 identified as protopine. The second substance MN-2 was also subjected to MS and NMR structural studies and identified as allokryptopine. Both alkaloids were previously isolated from Chelidonium majus. The both isolated substances were subjected to studies on their inhibitory activity against human erythrocyte acetylcholinesterase and human serum butyrylcholinesterase. Values were determined (protopine: IC50 (AChE) = 423 ± 12,7 µM, IC50 (BuChE) = 322 ± 9,6 µM, allokryptopine: IC50 (AChE) = 250 ± 7,5 µM, IC50 (BuChE) = 530 ± 15,9 µM). Both alkaloids showed low activity in comparison. With standard alkaloid...
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Biological activity of plants metabolites. XIX. Alkaloids of Peumus boldus MOL.
Bakyta, Matej ; Opletal, Lubomír (advisor) ; Cahlíková, Lucie (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Botany and Ecology Candidate: Matej Bakyta Consultant: Doc. RNDr. Lubomír Opletal, CSc. Title of Diploma Thesis: Biological activity of plants metabolites. XIX. Alkaloids of Peumus boldus MOL. A chloroform extract (pH 9-10, tertiary alkaloidal bases) was prepared from the leaves of Peumus boldus Mol. Processing of this extract by column chromatography and subsequent crystallization of fractions 34-39 led to the isolation of a compound named MB-1. The compound was identified as an aporphine alkaloid (+)-isocorydine (m. t. 183-184 řC) on the basis of results of spectral analysis (MS and NMR studies) and their comparison with literature. The isolated compound was tested for human blood acetylcholinesterase (AChE) and human plasma butyrylcholinesterase (BuChE) inhibition activity and for antioxidative activity (DPPH test). (+)-Isocorydine did not show significant human cholinesterase inhibition activity (AChE: IC50 >1000 μM; BuChE: IC50 = 657,1 μM) in comparison with reference compounds and did not show significant antioxidative effect in DPPH test (EC50 >1000 μM) in comparison with reference antioxidants. Key words: Peumus boldus, (+)-isocorydine, acetylcholinesterase, butyrylcholinesterase, antioxidative...
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