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Molecules 2018, 23(7), 1532; https://doi.org/10.3390/molecules23071532

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

1
Grup de Productes Naturals, Departament de Biologia, Sanitat i Medi Ambient, Facultat de Farmàcia, Universitat de Barcelona, 08028 Barcelona, Spain
2
Grupo de Investigación en Sustancias Bioactivas, Facultad de Ciencias Farmacéuticas y Alimentarias, Universidad de Antioquia UdeA, Calle 70 No, 52-21, Medellín 050010, Colombia
3
Departamento de Ciencias Básicas, Universidad Católica Luis Amigó, SISCO, Transversal 51A No. 67B-90, Medellín 050034, Colombia
4
Laboratorio de Cultivo Celular, Facultad de Ciencias de la Salud, Universidad de Talca, Talca 3460000, Chile
5
Laboratorio de Química de Productos Naturales, Instituto de Química de Recursos Naturales, Universidad de Talca, Talca 3460000, Chile
6
Programa de Investigación de Excelencia Interdisciplinaria en Química y Bio-orgánica de Recursos Naturales (PIEI-QUIM-BIO), Universidad de Talca, Talca 3460000, Chile
*
Author to whom correspondence should be addressed.
Academic Editor: John C. D’Auria
Received: 5 June 2018 / Revised: 18 June 2018 / Accepted: 19 June 2018 / Published: 26 June 2018
(This article belongs to the Special Issue Advances in Plant Alkaloid Research)
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Abstract

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 (IC50: 5.78 and 3.62 μg/mL, respectively) and BuChE (IC50: 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. View Full-Text
Keywords: Rhodophiala; alkaloids; molecular docking; AChE; BuChE; GC-MS Rhodophiala; alkaloids; molecular docking; AChE; BuChE; GC-MS
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).
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Tallini, L.R.; Bastida, J.; Cortes, N.; Osorio, E.H.; Theoduloz, C.; Schmeda-Hirschmann, G. Cholinesterase Inhibition Activity, Alkaloid Profiling and Molecular Docking of Chilean Rhodophiala (Amaryllidaceae). Molecules 2018, 23, 1532.

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