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Cytotoxic activity of selected Narcissus cultivars in vitro.
Maršálková, Aneta ; Hradiská Breiterová, Kateřina (advisor) ; Jošt, Petr (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Pharmacognosy and Pharmaceutical Botany (16-16230) Author: Aneta Maršálková Supervisor: PharmDr. Kateřina Hradiská Breiterová, Ph.D. Title of thesis: Cytotoxic activity of selected Narcissus cultivars in vitro. Key words: Narcissus, Amaryllidaceae alkaloids, cytotoxicity, HepG2 The main focus of this diploma thesis is the screening of summary alkaloidal extracts of selected cultivars of the genus Narcissus for their cytotoxic activity against HepG2 liver carcinoma cell line. In the second phase, the cytotoxic activity of the majorly represented Amaryllidaceae alkaloids (AmA) was screened, followed by an IC50 value determination. All studied alkaloidal extracts underwent also GC-MS and GC-FID qualitative and quantitative analysis to identify as many alkaloids as possible. A total of 23 alkaloids, namely 11,12-didehydroanhydrolycorine, 1-O-acetyl-10-norpluviine, 9-O-methylpseudolycorine, anhydropseudolycorine, assoanine, dehydroassoanine, dihydrolycorine, epi-norgalanthamine, galanthamine, galanthine, haemanthamine, hippeastrine, incartine, caranine, lycoramine, lycoraminone, lycorine, narwedine, norpluviine, pluviine, pseudolycorine, sanguinine, tazettine and several unspecified alkaloids of the homolycorine structural type were...
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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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Induction of oxidative stress in skin keratinocyte cells
Martínková, Nikola ; Jirkovská, Anna (advisor) ; Hradiská Breiterová, Kateřina (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences Student: Nikola Martínková Supervisor: PharmDr. Anna Jirkovská, Ph.D. Consultant: Mgr. Petr Jošt, Ph.D. Title of diploma thesis: Induction of oxidative stress in skin keratinocyte cells Keratinocytes are part of the epidermis and represent the majority of cells in the upper layer of human skin. When these cells are damaged by mutagenic substances, changes in the composition of the genetic material may occur, and even cell death may occur. Such substances that induce changes in DNA and have mutagenic potential include the chemical warfare agent sulfur mustard. The purpose of this study was to compare the HaCaT keratinocyte cell line with the experimentally derived 3HSM4 cell line in response to hydrogen peroxide-induced oxidative stress. The 3HSM4 cells were prepared by selecting resistant clones of HaCaT cells that were repeatedly exposed to the cytotoxic effects of sulfur mustard. The results of the comparison show that 3HSM4 cells proved to be more resistant to hydrogen peroxide. When glutathione (GSH) synthesis was blocked in both cell types, the cytotoxic effect of hydrogen peroxide was the same. Although 3HSM4 cells were shown to be more resistant in terms of cytotoxicity, they were found to have much...
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Isolation of alkaloids of the species Geissospermum vellosii Allemão and study of their biological activity VII.
Strašková, Veronika ; Šafratová, Marcela (advisor) ; Hradiská Breiterová, Kateřina (referee)
Strašková, V.: Isolation of alkaloids of the species Geissospermum vellosii Allemão and study of their biological activity VII. Diploma thesis, Charles University, Pharmaceutical Faculty in Hradec Králové, Department of pharmacognosy and pharmaceutical botany, Hradec Králové 2023, 75 s. Key words: Geissospermum vellosii, bark, alkaloidal extracts, isolation of alkaloids, GC/MS analysis, biological activity, acetylcholinesterase, butyrylcholinesterase. The main goal of this diploma thesis was isolation of pure alkaloids from the stem bark of Geissospermum vellosii and test their biological activity. G. vellosii is a South American tree from the Apocynaceae family. It is used in traditional medicine for various pathological conditions (e.g., bacterial, inflammatory, and fungal diseases). Indole alkaloids isolated from the stem bark of this tree exhibit significant biological activities such as antineoplastic, antimalarial, and anticholinesterase activities. For processing, the GV-2, GV-7-D, and GV-4-F fractions were selected in this diploma thesis. These fractions were obtained in previous studies from the original alkaloid extract of the stem bark, which showed interesting inhibitory activity against AchE and BuChE (AChE: IC50 = 15,19±0,96 µg/ml, BuChE: IC50 = 0,37±0,049 µg/ml). Four alkaloids,...
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Isolation of alkaloids of the species Geissospermum vellosii Allemão and study of their biological activity II.
Václavíková, Kateřina ; Šafratová, Marcela (advisor) ; Hradiská Breiterová, Kateřina (referee)
Václavíková, K., Isolation of alkaloids of the species Geissospermum vellosii Allemão and study of their biological activity II., Diploma thesis, Charles University, Faculty of Pharmacy in Hradec Králové, Department of Pharmacognosy, Hradec Králové 2020. The genus Geissospermum growing in South Amerika is important for phytochemistry because it contains indole alkaloids. This southamerican tree is in traditional treatment used for therapy of different diseases such as cognitive disorders, malaria or therapy of cancer. This plant was chosen for next investigation because of screening study that has shown very interesting activity against cholinesterases (IC50 AChE = 10.51 ± 3.03 μg/ml a IC50 BuChE = 0.39 ± 0.057 μg/ml). The aim of this study was to get summary extract from the stem bark, its processing, isolation of at least one pure alkaloid and definition of its structure. Thanks to chromatographic methods the alkaloid extract was separated into 16 fractions, which were processed afterwards. The isolation of alkaloids was from the fraction GV-8, which was separated by flash chromatography and following purification of isolated alkaloids by thin layer chromatography. The only pure alkaloid was isolated form this fraction (vellosimine), in which was tested the inhibition activity against human...
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Vinca minor L. alkaloids and their biological activity III.
Valová, Dominika ; Chlebek, Jakub (advisor) ; Hradiská Breiterová, Kateřina (referee)
Valová D.: Vinca minor L. alkaloids and their biological activity III. Diploma thesis, Charles University, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany, Hradec Králové, 2020, 75 p. Alzheimer's disease (AD) is a progressive, neurodegenerative disorder and it's the most common form of dementia. Because we're still not able to treat the cause of disease, searching for a new substance is relevant. This thesis is focused on isolation of alkaloids from a Vinca minor L. alkaloidal extract as a potential drug. The preparation and column chromatography of the summary extract were performed by Ing. Miroslav Ločárek as a part of his doctoral studies. Subsequent preparative TLC led to the isolation of three compounds. The chemical structures of the isolated alkaloids were elucidated by means of optical rotation, NMR and MS analyses and by comparison of the obtained data with those in the literature. One of the compounds was determined as(-)-vincine, other two compounds have not been isolated yet. Isolated compounds were also tested for their biological activity. Vincine, DV-1 a DV-3 were tested for their ability to inhibit acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). Additionally, vincine and DV-3 were also tested for their inhibitory activity on prolyl...
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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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Isolation of alkaloids from Hippeastrum ferrari and their biological activity
Buchalová, Tereza ; Suchánková, Daniela (advisor) ; Hradiská Breiterová, Kateřina (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Pharmacognosy and Pharmaceutical Botany Candidate: Tereza Buchalová Supervisor: PharmDr. Daniela Hulcová, Ph.D. Title of Thesis: Isolation of alkaloids from Hippeastrum cv. Ferrari and their biological activity Many different species, varieties, and cultivars of the genus Hippeastrum are popular indoor ornamental plants, but they also represent a rich source of important secondary metabolites called Amaryllidaceae alkaloids. These structurally unique compounds are known for their wide spectrum of biological activities such as anticancer, antiviral, and inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) which represent important part in therapy of Alzheimer's disease (AD). AD is a neurodegenerative disease that is identified as one of the most frequent causes of dementia in the world. Deficit of the neurotransmitter acetylcholine (ACh) in the cortex participates on the development of the AD, which results in the damage of cholinergic functions, and this is responsible for the memory loss and behavioural changes. AChE and BChE are enzymesinvolved in the termination of impulse transmission by rapid hydrolysis of ACh. Therefore, AChE and BChE inhibitors are nowadays the most important goal in...
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Alkaloids of Papaver rhoeas L. (Papaveraceae) and their biological activity related to Alzheimerʼs disease IV.
Gergely, Eszter ; Chlebek, Jakub (advisor) ; Hradiská Breiterová, Kateřina (referee)
Gergely, E.: Alkaloids of Papaver rhoeas L. (Papaveraceae) and their biological activity related to Alzheimerʼs disease IV. Diploma thesis, Charles University, Faculty of Pharmacy in Hradec Králové, Department of Pharmacognosy and Pharmaceutical Botany, Hradec Králové 2022, 61 pages. A chloroform alkaloid extract of aerial parts of Papaver rhoeas L. (Papaveraceae) showed a significant inhibitory activity on human butyrylcholinesterase (IC50hBuChE = 3,94 ± 0,35 µg/ml) [1,2]. hBuChE represents a key enzyme playing an important role in the pathogenesis of Alzheimer's disease. The main aim of this study was to isolate pure alkaloids by bio-guided assay using flash chromatography and preparative TLC, elucidate their structures (MS, NMR, and optical rotation) and cholinesterase inhibitory activity with Ellman's spectrophotometric method. Prediction of possibility of the molecules' crossing through blood-brain barrier (BBB) via logBB was calculated. Potential non-cytotoxicity of the most active compound was screened on selected nine cancer cell lines and one non-cancer cell line MRC-5. The identified isolated alkaloid (+)-caaverine showed a promising and selective hBuChE inibition (IC50hBuChE = 4,09 ± 0,50 µM and IC50hAChE > 100 µM, respectively) and should be able to cross the BBB (logBB = 0,372) by...
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Alkaloids of Narcissus species cultivars and their biological activity III.
Kahovcová, Anna ; Hradiská Breiterová, Kateřina (advisor) ; Suchánková, Daniela (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department: Department of Pharmacognosy and Pharmaceutical Botany Author: Kahovcová Anna Supervisor: PharmDr. Kateřina Hradiská Breiterová, PhD. Title of thesis: Alkaloids of Narcissus species cultivars and their biological activity III. Key words: Narcissus, alkaloids, biological activity, Alzheimer's disease, cytotoxicity The most important aim of this diploma thesis was to prepare summary alkaloid extracts from bulbs of the genus Narcissus L., specifically from seven cultivars Narcissus cv. MONDRAGON, RIP VAN WINKLE, SAGITTA, CHEERFULNESS, DOUBLE FASHION, PRECOCIOUS and FLOWER DRIFT, which were labeled as AL-458, AL-575, AL-443, AL-466, AL-549, AL-545 a AL-546. Samples were subsequently prepared for GC-MS analysis and screening determination of biological activities, namely the ability to inhibit human cholinesterases hAChE and hBuChE and cytotoxicity from these extracts. Using GC-MS analysis a total of 20 alkaloids were identified by comparing their mass spektra with the literature or the NIST library. Identified alkaloids include lycorine, lycoramine, lycoraminone, anhydrolycorine, pankracine, caranine, O-acetyllycorine, pluvine, norpluvine, assoanine, haemanthamine, galanthine, incartine, O-methylpseudolycorine, hippeastrine,...
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