Alzheimer's disease is an age-related, neurodegenerative disorder, characterized by cognitive impairment and restrictions in activities of daily living. This disease is the most common form of dementia with complex multifactorial pathological mechanisms. Many therapeutic approaches have been proposed. Among them, inhibition of acetylcholinesterase, butyrylcholinesterase, and prolyl oligopeptidase can be beneficial targets in the treatment of Alzheimer's disease. Roots, along with aerial parts of Argemone platyceras, were extracted with ethanol and fractionated on an alumina column using light petrol, chloroform and ethanol. Subsequently, repeated preparative thin-layer chromatography led to the isolation of (+)-laudanosine, protopine, (-)-argemonine, allocryptopine, (-)-platycerine, (-)-munitagine, and (-)-norargemonine belonging to pavine, protopine and benzyltetrahydroisoquinoline structural types. Chemical structures of the isolated alkaloids were elucidated by optical rotation, spectroscopic and spectrometric analysis (NMR, MS), and comparison with literature data. (+)-Laudanosine was isolated from A. platyceras for the first time. Isolated compounds were tested for human blood acetylcholinesterase, human plasma butyrylcholinesterase and recombinant prolyl oligopeptidase inhibitory activity. The alkaloids inhibited the enzymes in a dose-dependent manner. The most active compound (-)-munitagine, a pavine alkaloid, inhibited both acetylcholinesterase and prolyl oligopeptidase with IC50 values of 62.3 ± 5.8 µM and 277.0 ± 31.3 µM, respectively.

• Klíčová slova
• Alzheimer’s disease, Argemone platyceras, acetylcholinesterase, alkaloids, butyrylcholinesterase, prolyl oligopeptidase,
• MeSH
• alkaloidy chemie   izolace a purifikace   farmakologie   MeSH
• Alzheimerova nemoc farmakoterapie   MeSH
• Argemone chemie   MeSH
• butyrylcholinesterasa účinky léků   MeSH
• cholinesterasy účinky léků   MeSH
• chromatografie na tenké vrstvě metody   MeSH
• enzymatické testy metody   MeSH
• inhibiční koncentrace 50 MeSH
• inhibitory enzymů chemie   farmakologie   MeSH
• kořeny rostlin chemie   MeSH
• lidé MeSH
• magnetická rezonanční spektroskopie metody   MeSH
• objevování léků MeSH
• prolyloligopeptidasy MeSH
• rostlinné extrakty chemie   MeSH
• serinové endopeptidasy účinky léků   MeSH
• vztah mezi dávkou a účinkem léčiva MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• alkaloidy MeSH
• butyrylcholinesterasa MeSH
• cholinesterasy MeSH
• inhibitory enzymů MeSH
• PREPL protein, human MeSH Prohlížeč
• prolyloligopeptidasy MeSH
• rostlinné extrakty MeSH
• serinové endopeptidasy MeSH