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Natural compounds potentially influencing neurodegenerative diseases
Mňuková, Daniela ; Opletal, Lubomír (advisor) ; Suchánková, Daniela (referee)
Mňuková D.: Natural compounds potentially influencing neurodegenerative diseases. Diploma thesis, Charles University in Prag, Faculty of Pharmacy in Hradec Králové, Department os Pharmacognosy and Pharmaceutical botany, Hradec Králové 2022, 88 s. This research diploma thesis draws mainly from foreign professional literature. It provides an overview of important natural substances that potentially influence neurodegenerative diseases. The first part describes the moct common neurodegenerative diseases, their characteristics, epidemiology, pathogenesis and clinical picture. These diseases include Alzheimer's disease, Parkinson's disease, Lewy body dementia, multisystem atrophy, Pick's disease and other tauopathies, Huntington's disease, spinocerebellar ataxia and amyotrophic latelar sclerosis. The second part of diploma thesis presents natural substances that have been studied in preclinical and clinical studies in the last two decades for their potential to positively affect neurodegenerative diseases. The last part discusses the contribution of these natural substances fot therapy and prevention of neurodegenerative diseases. Keywords: neurodegenerative diseases, natural compounds, Alzheimer's disease, bioactive compounds
Screening of biological activity of various species of the genus Narcissus sp. II
Saaková, Franciska ; Suchánková, Daniela (advisor) ; Opletal, Lubomír (referee)
Charles Univerzity, Faculty of Pharmacy in Hradec Králové Department: Department of Pharmacognosy and Pharmaceutical botany Author: Franciska Saaková Supervisor: PharmDr. Daniela Hulcová Ph.D. Title of thesis: Screening of biological aktivity of various species of the genus Narcissus sp. II Key words: Narcissus, Daydream (AL-723), Gay Kybo (AL-725), High Society (AL728), Love Call (AL-734), Peach and Cream (AL-739), Sunny Girlfriend (AL-743) a Yellow Salome (AL-745), inhibition of the AChE and BuChE For thousands of years, plants in the Amaryllidaceae family have been used as a source of medicinal remedies. Already in the fourth century B.C., Hippocrates of Cos used oil from the daffodil Narcissus poeticus, for the treatment of uterine tumors. In addition to the already mentioned antitumor activity, this family has a number of other important biological effects such as antimalarial, antifungal, antibacterial, antiviral, emetic, analgesic, acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory effects [11]. This broad spectrum of properties makes them suitable candidates for the treatment of neurodegenerative diseases, cancer or malaria, whose incidence in the population is increasing. For this reason, it is very important to search for new potential drugs that could find...
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...
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...
Biological activity of macromycetes - A
Zvonková, Lenka ; Macáková, Kateřina (advisor) ; Opletal, Lubomír (referee)
Zvonková, L. Biological activity of macromycetes - A. Charles University in Pragu, Faculty of Pharmacy in Hradec Králové, 96 pp. Key words: mushrooms, compounds, free radicals, thin-layer chromatography (TLC), antioxidant activity, sequential injection analysis (SIA) Fourteen different mushrooms taxons (orders − Boletales, Pezizales, Polyporales and Russulales) were examined in this diploma thesis. Lyophiziled extracts were prepared under the precise set of conditions from the fruiting bodies and consequently used for recognition of compounds groups and for antioxidant activity detection. Thin-layer chromatography (TLC) was used for the determination of compounds groups. This TLC process proceeded in ascending development in pre-saturated chambers. From TLC results it was detected that tested mushrooms extracts contained especially amino-acids, saccharides, carboxylic acids, phenolic substances, sterols, which corresponds with the available literature. Alkaloids were also detected, especially in Leccinum griseum (Quél.) Singer extract. Antioxidant activity was set using sequential injection analysis method (SIA), which is based on DPPH radical bleaching. This method is very suitable, due to its rapidness and sensitivity, for evaluation of multiplicity routine antioxidant activity screenings. The...
Phytochemical study of Helianthus annuus L. IV
Podlipná, Jana ; Karlíčková, Jana (advisor) ; Opletal, Lubomír (referee)
Podlipná, J. Phytochemical study of Helianthus annuus L. IV. Diploma thesis 2008. Charles University in Prague, Faculty of Pharmacy in Hradec Králové, 93 pp. The thesis was focused on phytochemical research of plant Helianthus annuus L. The aim of the research was to obtain new information about plant metabolites of sunflower. There was an effort to evaluate the quality of included compounds in sprouts and sunflower seed shells and to divide ethanolic extract from leaves of this plant. Finally the evaluation of biological activity was done from fractions of leaves and shells. There weren't detected any alkaloids in extract from sprouts. Caffeic acid was detected in sunflower seed shells according to thin-layer chromatography. 80% ethanolic extract from sunflower leaves had significant antioxidant activity which was measured both by DPPH radical and FRAP method. Fat acids were found in fraction No. 14 (from 2nd chromatographic column of extract from leaves). Extract from leaves was toxic for worms Tubifex tubifex Müll. but it wasn't phototoxic.
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....
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...
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...
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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