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Screening of biological activity of various species of the genus Narcissus sp. IV
Valešová, Zuzana ; Suchánková, Daniela (advisor) ; Vrabec, Rudolf (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department: Department of Pharmacognosy and Pharmaceutical botany Author: Zuzana Valešová Supervisor: PharmDr. Daniela Suchánková, Ph.D. Title of thesis: Screening of biological activity of various species of the genus Narcissus sp. IV Key words: Narcisus sp., bulbs, alkaloidal extracts, GC/MS analysis, biological activity, acetylcholinesterase, butyrylcholinesterase Plants of the family Amaryllidaceae have a long history of using as traditional remedies. Plants of this family produce structurally unique isoquinoline compounds, which have been called "Amaryllidaceae alkaloids". Over 600 Amaryllidaceae alkaloids have been isolated, which are characterized by interesting biological activity. Cytotoxic, antimicrobial, antiparasitic, anti-inflammatory activity has been described, but the best known is the inhibitory activity against the enzymes acetylcholinesterase and butyrylcholinesterase, which is used in practice for therapy of Alzheimer's disease. [8, 9] The genus Narcissus is primarily known as decorative plants that blooms in early spring. However, daffodils are also used to isolate galanthamine or other alkaloids that are being studied for their effect. [13] The aim of this thesis was to screen the biological activity of extracts of the...
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Isolation of alkaloid galanthin from Narcissus poeticus recurvus and its semi-synthetic derivatives
Lojkásek, Matěj ; Suchánková, Daniela (advisor) ; Kučera, Tomáš (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacognosy Candidate: Matěj Lojkásek Instructor: Pharm.Dr. Daniela Hulcová, Ph.D. Title of thesis: Isolation of alkaloids from Narcissus poeticus recurvus and its semi-synthetic derivatives Key words: Amaryllidaceae, galanthin, semi-synthetic derivatives, Alzheimer's disease, acetylcholinesterase, butyrylcholinesterase, cytotoxicity. As part of the thesis, two alkaloid substances (galanthin and cherylline) were isolated from the bulbs of the mother plant Narcissus poeticus recurvus using preparative TLV chromatography. The obtained galanthin was subsequently used for the preparation of 6 derivatives of this alkaloid, namely esters. Galanthine esters were prepared by acylation of the hydroxyl group. The derivatives were identified by NMR, HMRS and the optical rotation was measured. In the end, only 5 of the prepared substances were recovered in sufficient quantity and purity. Derivative G2 could not be retained. In the case of G1, G4 and G6, the yield of the reaction was higher than 50%, whereas for G3 it was 49.55%, G2 19.23% and G5 39.79%. All prepared derivatives except G2 were tested for inhibitory activity against cholinesterases by the Ellman method using recombinant enzymes. Unfortunately, according to the IC50 values...
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Screening of biological activity of various species of the genus Narcissus sp. IV
Valešová, Zuzana ; Suchánková, Daniela (advisor) ; Vrabec, Rudolf (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department: Department of Pharmacognosy and Pharmaceutical botany Author: Zuzana Valešová Supervisor: PharmDr. Daniela Suchánková, Ph.D. Title of thesis: Screening of biological activity of various species of the genus Narcissus sp. IV Key words: Narcisus sp., bulbs, alkaloidal extracts, GC/MS analysis, biological activity, acetylcholinesterase, butyrylcholinesterase Plants of the family Amaryllidaceae have a long history of using as traditional remedies. Plants of this family produce structurally unique isoquinoline compounds, which have been called "Amaryllidaceae alkaloids". Over 600 Amaryllidaceae alkaloids have been isolated, which are characterized by interesting biological activity. Cytotoxic, antimicrobial, antiparasitic, anti-inflammatory activity has been described, but the best known is the inhibitory activity against the enzymes acetylcholinesterase and butyrylcholinesterase, which is used in practice for therapy of Alzheimer's disease. [8, 9] The genus Narcissus is primarily known as decorative plants that blooms in early spring. However, daffodils are also used to isolate galanthamine or other alkaloids that are being studied for their effect. [13] The aim of this thesis was to screen the biological activity of extracts of the...
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Screening of biological activity of various species of the genus Narcissus sp. III
Růžičková, Zuzana ; Suchánková, Daniela (advisor) ; Chlebek, Jakub (referee)
CharlesUniversity,FacultyofPharmacyinHradecKrálové Department: DepartmentofPharmacognosyandPharmaceuticalbotany Author: Zuzana Růžičková Supervisor: PharmDr.DanielaSuchánková,Ph.D. Title of thesis: Screeningofbiologicalactivityofvariousspeciesofthe genusNarcissussp.III Key words: Narcissus sp., bulbs, alkaloidal extracts, GC/MS analysis, biological activity, acetylcholinesterase,butyrylcholinesterase Alzheimer'sdiseaseisaseverediseasethatrepresentsthemostcommoncauseofdementiaanddeath. Thedisease ischaracterized bya decrease off nerve cells and brain tissue.Forpatientswith Alzheimer's disease, memory lapses are typical, at the beginning of the disease states of anxiety and depression occur.The main cause isthe formation and deposition of β-amyloid and deficit of the neurotransmitter acetylcholine. Unfortunately, we do not know how to cure the Alzheimer's disease, but we can significantly slow it down by prolonging themild stages of the disease. Treatment is mainly directed to AChEinhibitorstoeliminateACHdeficiency. The main goal of this diploma thesis was to obtain summary alkaloid extracts from bulbs of seven cultivars of the genus Narcissus sp., which could have been a potential source of substances for the treatment of Alzheimer's disease. Cultivars were specifically Narcissus cv. Banana Splash,...
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Derivatives of Amaryllidaceae alkaloids as potential drugs in the treatment of tumor diseases
Valachová, Iva ; Suchánková, Daniela (advisor) ; Kučera, Tomáš (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacognosy Candidate: Iva Valachová Supervisor: Pharm.Dr. Daniela Hulcová, Ph.D. Title of diploma thesis: Derivatives of Amaryllidaceae alkaloids as potential drugs in the treatment of tumor diseases Twelve aromatic derivatives were prepared. The substitutions were performed on the hydroxyl group at C-3. This was acylated with differently substituted benzoyl chlorides affording the corresponding esters. Structural identification was performed by 1D- and 2D- NMR, ESI-HRMS spectroscopic techniques and optical rotation measurement. The yield of all reactions was more than 60 %. After converting these derivatives to hydrochlorides, their biological activity was tested. The Amaryllidaceae alkaloid vittaine itself exhibits cytotoxic activity and therefore its derivatives have been investigated in this respect. It has been tested against 9 cancerous and 1 non-cancerous cell lines. 3-O-(4-Chloro-3-nitrobenzoyl)vittatine showed the highest cytotoxic activity, unfortunatelly, it does not selectively affect only cancerous cells. Conversely, 3-O-(2-naphthoyl)vittatine has a selective effect on the HT-29 cancerous cell line (colorectal carcinoma) with a viability value of 32 ± 3 %, potentially being the subject of further studies of cytotoxicity...
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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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Amaryllidaceae alkaloids as model structures for the development of new potential drugs
Knápková, Soňa ; Suchánková, Daniela (advisor) ; Cahlíková, Lucie (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacognosy Candidate: Soňa Knápková Supervisor: PharmDr. Daniela Hulcová, Ph.D. Title of diploma thesis: Amaryllidaceae alkaloids as model structures for the development of new potential drugs The family Amaryllidaceae includes a large number of genus of flowering plants as Hippeastrum, Narcissus or Zephyrantes. All of them contain specific Amaryllidaceae alkaloids, which are characteristic of this family due to their chemical structures. The discovery and study of these alkaloids has attracted the attention of many scientists due to the diverse biological activity of these compounds, such as cytotoxic, anticholinesterases, antibacterial and antiviral effects. Plants of the genus Hippeastrum have been used in traditional medicine to treat tumors and inflammatory disorders. This use can be explained by the alkaloids, which it contains. It is mainly lycorine, haemanthamine and pancristatine. These compounds have an antitumor effect. The species Hippeastrum cv. Ferrari is further rich in the alkaloid vittatine. In some research, the simple semisynthetic derivatives of haemanthamine displayed promising inhibitory activities against cholinesterases. For this reason, vittatine was chosen as next lead-structure, for preparation of...
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Biological activity evaluation of substances of natural origin I.
Kupčíková, Júlia ; Suchánková, Daniela (advisor) ; Kučera, Tomáš (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmacognosy and Pharmaceutical botany Candidate: Júlia Kupčíková Supervisor: PharmDr. Daniela Suchánková, Ph.D. Title of diploma thesis: Biological activity evaluation of substances of natural origin I. Alzheimer's disease (AD) is progressive neurodegenerative brain disorder characterized by memory loss and cognitive impairments. Manifestation of this disease is associated with decreased level of acetylcholine. Current treatment of AD is symptomatic and involves mainly restoring of acetylcholine levels through cholinesterase inhibition. Galanthamine, one of acetylcholinesterase inhibitors indicated for the treatment of AD belongs to Amaryllidaceae alkaloids. Therefore, other Amaryllidaceae alkaloids and their derivatives are prepared and studied for similar inhibitory properties. Amaryllidaceae alkaloid vittatine does not have cholinesterase inhibitory properties, but previous findings proved that some vittatine derivatives have potency to inhibit both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). Seven new semisynthetic derivatives of vittatine were prepared and studied for their inhibitory potential against both cholinesterases, using the Ellman's method. Significant BuChE inhibitory activity was...
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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
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Screening of biological activity of various species of the genus Narcissus sp. I
Komendová, Karolína ; Suchánková, Daniela (advisor) ; Chlebek, Jakub (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Pharmacognosy and Pharmaceutical botany Candidate: Karolína Komendová Supervisor: PharmDr. Daniela Hulcová, Ph.D. Title of thesis: Screening of biological activity of various species of the genus Narcissus sp. I Key words: Amaryllidaceae, Narcissus, alkaloids, AChE, BuChE, Alzheimer's disease Alkaloids from family Amaryllidaceae (AA) nowadays belong to the most important and also the most examined alkaloids. This is because of their structural diversity and a broad spectrum of biological effects. The main aim of my diploma was to prepare whole bulb extracts from seven different cultivated varieties of genus Narcissus and to select those with the highest potential to inhibit enzyme acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). Inhibition of these enzymes is very important in the treatment of Alzheimer's disease (AD). Summary extracts were obtained from these cultivars: N. cv, Apotheose (AL - 718), N. cv. Chromacolor (AL - 722), N. cv. Hungarian Rhapsody (AL - 729), N. cv. Mon Cheri (AL - 736), N. cv. Peach Cobbler (AL - 738), N. cv. Pink Pride (AL - 740) a N. cv. Red Devon (AL - 742). The isolated extracts were subsequently analyzed by GC-MS. The following alkaloids were found in the majority of extracts:...
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