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Chemical Profiling and Cholinesterase Inhibitory Activity of Five Phaedranassa Herb. (Amaryllidaceae) Species from Ecuador

It is estimated that 50 million people in the world live with dementia, 60–70% of whom suffer from Alzheimer’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 exclusiv...

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Autores principales: Moreno, Raúl, Tallini, Luciana R., Salazar, Cristina, Osorio, Edison H., Montero, Evelin, Bastida, Jaume, Oleas, Nora H., Acosta León, Karen
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7248819/
https://www.ncbi.nlm.nih.gov/pubmed/32365796
http://dx.doi.org/10.3390/molecules25092092
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author Moreno, Raúl
Tallini, Luciana R.
Salazar, Cristina
Osorio, Edison H.
Montero, Evelin
Bastida, Jaume
Oleas, Nora H.
Acosta León, Karen
author_facet Moreno, Raúl
Tallini, Luciana R.
Salazar, Cristina
Osorio, Edison H.
Montero, Evelin
Bastida, Jaume
Oleas, Nora H.
Acosta León, Karen
author_sort Moreno, Raúl
collection PubMed
description It is estimated that 50 million people in the world live with dementia, 60–70% of whom suffer from Alzheimer’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.
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spelling pubmed-72488192020-06-10 Chemical Profiling and Cholinesterase Inhibitory Activity of Five Phaedranassa Herb. (Amaryllidaceae) Species from Ecuador Moreno, Raúl Tallini, Luciana R. Salazar, Cristina Osorio, Edison H. Montero, Evelin Bastida, Jaume Oleas, Nora H. Acosta León, Karen Molecules Article It is estimated that 50 million people in the world live with dementia, 60–70% of whom suffer from Alzheimer’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. MDPI 2020-04-30 /pmc/articles/PMC7248819/ /pubmed/32365796 http://dx.doi.org/10.3390/molecules25092092 Text en © 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Moreno, Raúl
Tallini, Luciana R.
Salazar, Cristina
Osorio, Edison H.
Montero, Evelin
Bastida, Jaume
Oleas, Nora H.
Acosta León, Karen
Chemical Profiling and Cholinesterase Inhibitory Activity of Five Phaedranassa Herb. (Amaryllidaceae) Species from Ecuador
title Chemical Profiling and Cholinesterase Inhibitory Activity of Five Phaedranassa Herb. (Amaryllidaceae) Species from Ecuador
title_full Chemical Profiling and Cholinesterase Inhibitory Activity of Five Phaedranassa Herb. (Amaryllidaceae) Species from Ecuador
title_fullStr Chemical Profiling and Cholinesterase Inhibitory Activity of Five Phaedranassa Herb. (Amaryllidaceae) Species from Ecuador
title_full_unstemmed Chemical Profiling and Cholinesterase Inhibitory Activity of Five Phaedranassa Herb. (Amaryllidaceae) Species from Ecuador
title_short Chemical Profiling and Cholinesterase Inhibitory Activity of Five Phaedranassa Herb. (Amaryllidaceae) Species from Ecuador
title_sort chemical profiling and cholinesterase inhibitory activity of five phaedranassa herb. (amaryllidaceae) species from ecuador
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7248819/
https://www.ncbi.nlm.nih.gov/pubmed/32365796
http://dx.doi.org/10.3390/molecules25092092
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