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Cholinesterase Inhibition Activity, Alkaloid Profiling and Molecular Docking of Chilean Rhodophiala (Amaryllidaceae)

Amaryllidaceae plants are the commercial source of galanthamine, an alkaloid approved for the clinical treatment of Alzheimer’s disease. The chemistry and bioactivity of Chilean representatives of Rhodophiala genus from the family of Amaryllidaceae have not been widely studied so far. Ten collection...

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Autores principales: Tallini, Luciana R., Bastida, Jaume, Cortes, Natalie, Osorio, Edison H., Theoduloz, Cristina, Schmeda-Hirschmann, Guillermo
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6099557/
https://www.ncbi.nlm.nih.gov/pubmed/29949847
http://dx.doi.org/10.3390/molecules23071532
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author Tallini, Luciana R.
Bastida, Jaume
Cortes, Natalie
Osorio, Edison H.
Theoduloz, Cristina
Schmeda-Hirschmann, Guillermo
author_facet Tallini, Luciana R.
Bastida, Jaume
Cortes, Natalie
Osorio, Edison H.
Theoduloz, Cristina
Schmeda-Hirschmann, Guillermo
author_sort Tallini, Luciana R.
collection PubMed
description Amaryllidaceae plants are the commercial source of galanthamine, an alkaloid approved for the clinical treatment of Alzheimer’s disease. The chemistry and bioactivity of Chilean representatives of Rhodophiala genus from the family of Amaryllidaceae have not been widely studied so far. Ten collections of five different Chilean Rhodophiala were analyzed in vitro for activity against enzymes such as acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) as well as for their alkaloid composition by GC-MS. To obtain an insight into the potential AChE and BuChE inhibitory activity of the alkaloids identified in the most active samples, docking experiments were carried out. Although galanthamine was found neither in aerial parts nor in bulbs of R. splendens, these plant materials were the most active inhibitors of AChE (IC(50): 5.78 and 3.62 μg/mL, respectively) and BuChE (IC(50): 16.26 and 14.37 μg/mL, respectively). Some 37 known alkaloids and 40 still unidentified compounds were detected in the samples, suggesting high potential in the Chilean Amaryllidaceae plants as sources of both novel bioactive agents and new alkaloids.
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spelling pubmed-60995572018-11-13 Cholinesterase Inhibition Activity, Alkaloid Profiling and Molecular Docking of Chilean Rhodophiala (Amaryllidaceae) Tallini, Luciana R. Bastida, Jaume Cortes, Natalie Osorio, Edison H. Theoduloz, Cristina Schmeda-Hirschmann, Guillermo Molecules Article Amaryllidaceae plants are the commercial source of galanthamine, an alkaloid approved for the clinical treatment of Alzheimer’s disease. The chemistry and bioactivity of Chilean representatives of Rhodophiala genus from the family of Amaryllidaceae have not been widely studied so far. Ten collections of five different Chilean Rhodophiala were analyzed in vitro for activity against enzymes such as acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) as well as for their alkaloid composition by GC-MS. To obtain an insight into the potential AChE and BuChE inhibitory activity of the alkaloids identified in the most active samples, docking experiments were carried out. Although galanthamine was found neither in aerial parts nor in bulbs of R. splendens, these plant materials were the most active inhibitors of AChE (IC(50): 5.78 and 3.62 μg/mL, respectively) and BuChE (IC(50): 16.26 and 14.37 μg/mL, respectively). Some 37 known alkaloids and 40 still unidentified compounds were detected in the samples, suggesting high potential in the Chilean Amaryllidaceae plants as sources of both novel bioactive agents and new alkaloids. MDPI 2018-06-26 /pmc/articles/PMC6099557/ /pubmed/29949847 http://dx.doi.org/10.3390/molecules23071532 Text en © 2018 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
Tallini, Luciana R.
Bastida, Jaume
Cortes, Natalie
Osorio, Edison H.
Theoduloz, Cristina
Schmeda-Hirschmann, Guillermo
Cholinesterase Inhibition Activity, Alkaloid Profiling and Molecular Docking of Chilean Rhodophiala (Amaryllidaceae)
title Cholinesterase Inhibition Activity, Alkaloid Profiling and Molecular Docking of Chilean Rhodophiala (Amaryllidaceae)
title_full Cholinesterase Inhibition Activity, Alkaloid Profiling and Molecular Docking of Chilean Rhodophiala (Amaryllidaceae)
title_fullStr Cholinesterase Inhibition Activity, Alkaloid Profiling and Molecular Docking of Chilean Rhodophiala (Amaryllidaceae)
title_full_unstemmed Cholinesterase Inhibition Activity, Alkaloid Profiling and Molecular Docking of Chilean Rhodophiala (Amaryllidaceae)
title_short Cholinesterase Inhibition Activity, Alkaloid Profiling and Molecular Docking of Chilean Rhodophiala (Amaryllidaceae)
title_sort cholinesterase inhibition activity, alkaloid profiling and molecular docking of chilean rhodophiala (amaryllidaceae)
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6099557/
https://www.ncbi.nlm.nih.gov/pubmed/29949847
http://dx.doi.org/10.3390/molecules23071532
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