|
|
Amaryllidaceae alkaloids of montanine type and their derivatives as potential drugs.
Maafi, Negar ; Cahlíková, Lucie (advisor) ; Šmejkal, Karel (referee) ; Havlík, Jaroslav (referee)
Charles University, Faculty of Pharmacy in Hradec Králové Department of Pharmacognosy and Pharmaceutical Botany Candidate: Negar Maafi Supervisor: Prof. Ing. Lucie Cahlíková, Ph.D. Title of Doctoral Thesis: Amaryllidaceae alkaloids of montanine type and their derivatives as potential drugs. Based on the knowledge of the biological activity of montanine-type alkaloids of Amaryllidaceae, these alkaloids were selected for the preparation of their semisynthetic derivatives to study the relationship between structure and the activity. Derivatives of montanine-type alkaloids were prepared using haemanthamine and montanine as starting substances. The montanine-type alkaloid 3-O- methylpancracine was prepared using intramolecular rearrangement of haemanthamine. Previously isolated montanine from bulbs of Hippeastrum x hybridum cv. Ferrari was used in synthesize of derivatives. In total, more than 80 aliphatic and aromatic derivatives of montanine and 3-O- methylpancracine have been prepared. All compounds were identified using 1D- and 2D-NMR, MS, HRMS, and so forth. The prepared derivatives were screened for a wide range of biological activities (inhibitory potential against hAChE/hBuChE, antimycobacterial, antibacterial and antifungal activity, cytotoxicity, and others). In the hAChE/hBuChE study, the...
|
|
|
Alkaloids from Narcissus pseudonarcissus L. cv. Dutch Master and their cholinesterase and prolyl oligopeptidase inhibitory activity.
Farkašovský, Marek ; Chlebek, Jakub (advisor) ; Siatka, Tomáš (referee)
Farkašovský Marek: Alkaloids from Narcissus pseudonarcissus L. cv. Dutch Master and their cholinesterase and prolyl oligopeptidase inhibition activity. Rigorous thesis 2017, Charles university, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany and Ecology. The content of this work was isolation of minimum two compound from alkaloid fraction ND 3 - 5/2, obtained by column chromatography of Narcissus pseudonarcissus L. cv. Dutch Master alkaloid extract. Preparation of extract and its column chromatography was performed by Mgr. Daniela Hulcová as a part of her doctoral studies. Two different alkaloids were isolated with preparative TLC method. Their structure was determined with optical rotation, MS (EI, ESI), 1H NMR and 13C NMR analysis. Obtained data were compared with facts with those in literature. The first isolated compound was lycorine type alkaloid O-acetylpluvine. Its inhibition activity compared to positive standards (galanthamine, huperzine A, physostigmine, berberine and Z-pro-prolinal) was mild - IC50 AChE: 684 ± 54 µM, IC50 BuChE: 603 ± 49 µM, IC50 POP ˃1000 µM. From the point of its cholinesterase and POP inhibition, this results make O-acetylpluvine unusable compound in treatment of AD. The second isolated compound was a new alkaloid, which has not been...
|
|
|
Alkaloids from Narcissus pseudonarcissus L. cv. Dutch Master and their cholinesterase and prolyl oligopeptidase inhibitory activity.
Farkašovský, Marek ; Chlebek, Jakub (advisor) ; Siatka, Tomáš (referee)
Farkašovský Marek: Alkaloids from Narcissus pseudonarcissus L. cv. Dutch Master and their cholinesterase and prolyl oligopeptidase inhibition activity. Rigorous thesis 2017, Charles university, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany and Ecology. The content of this work was isolation of minimum two compound from alkaloid fraction ND 3 - 5/2, obtained by column chromatography of Narcissus pseudonarcissus L. cv. Dutch Master alkaloid extract. Preparation of extract and its column chromatography was performed by Mgr. Daniela Hulcová as a part of her doctoral studies. Two different alkaloids were isolated with preparative TLC method. Their structure was determined with optical rotation, MS (EI, ESI), 1H NMR and 13C NMR analysis. Obtained data were compared with facts with those in literature. The first isolated compound was lycorine type alkaloid O-acetylpluvine. Its inhibition activity compared to positive standards (galanthamine, huperzine A, physostigmine, berberine and Z-pro-prolinal) was mild - IC50 AChE: 684 ± 54 µM, IC50 BuChE: 603 ± 49 µM, IC50 POP ˃1000 µM. From the point of its cholinesterase and POP inhibition, this results make O-acetylpluvine unusable compound in treatment of AD. The second isolated compound was a new alkaloid, which has not been...
|
|
|
Neurotropic and antioxidative activity of some selected species of monocotyledonous alkaloidal plants in vitro. VIII.
Breiterová, Kateřina ; Cahlíková, Lucie (advisor) ; Ločárek, Miroslav (referee)
Author: Kateřina Breiterová Title: Neurotropic and antioxidative activity of some selected species of monocotyledonous alkaloidal plants in vitro. VIII. Diploma thesis Charles Univerzity in Prague, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany and Ecology 2015, 101 p. More than 50 % cases of dementia are nowadays caused byAlzheimer's disease (AD). AD is a progressive neurodegenerative disease and it causes gradual memory loss, disorientation and behavioral disorders which affect patient's social and occupational life. AD is characteristic by loss of neurons in some regions of brain - for example hippocampus and cortex. Ethiopathogenesis of this disease is not completely known - that is why the treatment is still just symptomatic. Formation of β-amyloid deposits in brain tissue plays an important role - it is a protein which creates extracellular plagues around neurites and causes their degeneration and death. Intracellular tangles are made up of the changed τ-protein. These tangles also cause death of the neuronal cell. The degeneration of neurons is supported by reactive oxygen radicals too. The another problem is a glutamatergic system disorder. This set of excitatory amino acids is important for correct long-term memory formation. Patients with AD suffer from...
|
guest ::
