Monoterpene indole alkaloids from Vinca minor L. (Apocynaceae): Identification of new structural scaffold for treatment of Alzheimer's disease
![Thumbnail](/bitstream/handle/20.500.14178/1705/Monoterpene_611439_22.pdf.jpg?sequence=5&isAllowed=y)
View/ Open
Date
2022Author
Vrabec, Rudolf
Maříková, Jana
Ločárek, Miroslav
Korábečný, Jan
Hulcová, Daniela
Hošťálková, Anna
Kuneš, Jiří
Chlebek, Jakub
Kučera, Tomáš
Hrabinová, Martina
Jun, Daniel
Soukup, Ondřej
Andrisano, Vincenza
Jenčo, Jaroslav
Šafratová, Marcela
Nováková, Lucie
Opletal, Lubomír
Cahlíková, Lucie
Metadata
Show full item recordAbstract (en)
One undescribed indole alkaloid together with twenty-two known compounds have been isolated from aerial parts of Vinca minor L. (Apocynaceae). The chemical structures of the isolated alkaloids were determined by a combination of MS, HRMS, 1D, and 2D NMR techniques, and by comparison with literature data. The NMR data of several alkaloids have been revised, corrected, and missing data have been supplemented. Alkaloids isolated in sufficient quantity were screened for their in vitro acetylcholinesterase (AChE; E.C. 3.1.1.7) and butyrylcholinesterase (BuChE; E.C. 3.1.1.8) inhibitory activity. Selected compounds were also evaluated for prolyl oligopeptidase (POP; E.C. 3.4.21.26), and glycogen synthase 3 beta-kinase (GSK-3 beta; E.C. 2.7.11.26) inhibition potential. Significant hBuChE inhibition activity has been shown by (-)-2-ethyl-3[2-(3-ethylpiperidinyl)-ethyl]-1H-indole with an IC50 value of 0.65 +/- 0.16 mu M. This compound was further studied by enzyme kinetics, along with in silico techniques, to reveal the mode of inhibition. This compound is also predicted to cross the blood-brain barrier (BBB) through passive diffusion.Permanent link
https://hdl.handle.net/20.500.14178/1705License
![Creative Commons Uveďte původ-Neužívejte dílo komerčně-Nezpracovávejte 4.0 International](/themes/ukuk_publications//images/creativecommons/cc-generic.png)