Chemical Profiling and Cholinesterase Inhibitory Activity of Five Phaedranassa Herb. (Amaryllidaceae) Species from Ecuador
Autor: | Raúl Moreno, Nora H. Oleas, Evelin Montero, Cristina Salazar, Edison Osorio, Luciana R. Tallini, Karen Acosta León, Jaume Bastida |
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Jazyk: | angličtina |
Rok vydání: | 2020 |
Předmět: |
food.ingredient
Aché Phaedranassa Pharmaceutical Science alkaloids 01 natural sciences Analytical Chemistry lcsh:QD241-441 03 medical and health sciences food Alkaloids lcsh:Organic chemistry Drug Discovery Alcaloides Physical and Theoretical Chemistry Butyrylcholinesterase 030304 developmental biology Cholinesterase chemistry.chemical_classification 0303 health sciences Traditional medicine biology 010405 organic chemistry Amaril·lidàcies Alkaloid Organic Chemistry Amaryllidaceae cholinesterases molecular docking Alzheimer's disease biology.organism_classification language.human_language 0104 chemical sciences Enzyme Malaltia d'Alzheimer chemistry Chemistry (miscellaneous) Herb language biology.protein Molecular Medicine GC-MS |
Zdroj: | Molecules Volume 25 Issue 9 Dipòsit Digital de la UB Universidad de Barcelona Molecules, Vol 25, Iss 2092, p 2092 (2020) |
ISSN: | 1420-3049 |
DOI: | 10.3390/molecules25092092 |
Popis: | It is estimated that 50 million people in the world live with dementia, 60&ndash 70% of whom suffer from Alzheimer&rsquo s disease (AD). Different factors are involved in the development of AD, including a reduction in the cholinergic neurotransmission level. The Amaryllidaceae plant family contains an exclusive, large, and still understudied alkaloid group characterized by a singular skeleton arrangement and a broad spectrum of biological activities. The chemistry and biodiversity of Ecuadorian representatives of the Phaedranassa genus (Amaryllidaceae) have not been widely studied. In this work, five Ecuadorian Phaedranassa species were examined in vitro for their activity towards the enzymes acetyl- (AChE) and butyrylcholinesterase (BuChE), and the alkaloid profile of bulb extracts was analyzed by GC-MS. The species Phaedranassa cuencana and Phaedranassa dubia showed the most AChE and BuChE inhibitory activity, respectively. To obtain insight into the potential role of the identified alkaloids in these inhibitory effects, docking experiments were carried out, and cantabricine showed in silico inhibitory activity against both cholinesterase structures. Our results show that Amaryllidaceae species from Ecuador are a potential source of new drugs for the palliative treatment of AD. |
Databáze: | OpenAIRE |
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