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Vinca minor L. alkaloids and their biological activity I.
Jurkaninová, Martina ; Chlebek, Jakub (advisor) ; Opletal, Lubomír (referee)
1 9 ABSTRACT Jurkaninová, M.: Vinca minor L. alkaloids and their biological activity I. Diploma thesis, Charles University, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany, Hradec Králové, 2019 The aim of this thesis was the isolation of alkaloids from selected fraction 3 (joined fractions (15 - 36), which was a sub-fraction of the fraction VM 323 - 327. It was obtained from the previous processing of an alkaloidal extract from the Vinca minor L at the Department of Pharmaceutical Botany as a part of elaboration of diploma thesis of Aneta Vítavcová.[78] The fraction VM 323-327 was separated by column chromatography on silica gel and a totally, of 7 subfractions were obtained. Subsequent repeated processing of the selected sub-fraction 3 (15 - 36) by preparative TLC on silica gel resulted in the isolation of (-)-vinoxine and its racemate (±)-vinoxine. Identification of their structure was determined based on MS, NMR and optical rotation. The inhibitory activity against acetylcholinesterase, butyrylcholiesterase and prolyl oligopeptidase were determined for the isolated substances. Inhibitory activity against selected enzymes was measured by spectrophotometric methods. Isolated alkaloids were required to be inactive against AChE and POP (IC50 >1000 μM), against to BChE showed a...
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Cytotoxic and cholinesterase inhibitory activity of extracts from selected species of the Centaurea L. genus
Faschingbauer, Jakub ; Chlebek, Jakub (advisor) ; Šafratová, Marcela (referee)
Faschingbauer J.: Cytotoxic and cholinesterase inhibitory activity of extracts from selected species of the Centaurea L. genus. Diploma thesis, Charles University, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany, Hradec Králové, 2019. During the screening of biologically active secondary metabolites of plants carried out at the Department of Pharmaceutical Botany FAF UK, selected taxa of the genus Centaurea (Asteraceae) were investigated. This study is focused on a basic phytohemical research of extracts prepared from Centaurea cyanus, Centaurea jacea, Centaurea scabiosa, Centaurea pseudophrygia, Centuarea stoebe, Centaurea solstitialis a Centaurea benedicta. Extracts were prepared for evidence of the proof reactions of TLC and MS analysis (EI, ESI) to clarify a potential presence of alkaloids. EtOAc and ethanol extracts were evaluated for potential inhibitory activity against human erythrocyte acetylcholinesterase (AChE) and plasma butyrylcholinesterase (BChE) and cytotoxicity against selected 9 tumor lines. C. cyanus alkaloid extract had interesting cholinesterase activity which selectively inhibited BChE (IC50 BChE = 22.62 ± 3.62 μg / ml, IC50 AChE = 221.50 ± 44.56 g / ml). Other EtOAc extracts of selected Centaurea species were considered inactive (IC50 > 100 μg/ml)....
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