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

1
Group of Natural Products, Faculty of Pharmacy, University of Barcelona, Av. Joan XXIII, 27-31, 08028 Barcelona, Spain
2
Faculty of Pharmacy, Federal University of Rio Grande do Sul, Av. Ipiranga 2752, Porto Alegre RS 90610-000, Brazil
3
Grupo de Investigación de Productos Naturales y Farmacia, Facultad de Ciencias, Escuela Superior Politécnica del Chimborazo, Panamericana Sur km 1 1/2, Riobamba EC060155, Ecuador
4
Facultad de Ciencias Naturales y Matemáticas, Universidad de Ibagué, Carrera 22 Calle 67, Ibagué 730001, Colombia
5
Centro de Investigación de la Biodiversidad y Cambio Climático (BioCamb) e Ingeniería en Biodiversidad y Recursos Genéticos, Facultad de Ciencias de Medio Ambiente, Universidad Tecnológica Indoamérica, Machala y Sabanilla, Quito EC170301, Ecuador
*
Author to whom correspondence should be addressed.
Academic Editor: John C. D’Auria
Molecules 2020, 25(9), 2092; https://doi.org/10.3390/molecules25092092
Received: 3 March 2020 / Revised: 13 April 2020 / Accepted: 21 April 2020 / Published: 30 April 2020
(This article belongs to the Special Issue Amaryllidaceae Alkaloids)
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. View Full-Text
Keywords: alkaloids; Amaryllidaceae; cholinesterases; GC-MS; molecular docking; Phaedranassa alkaloids; Amaryllidaceae; cholinesterases; GC-MS; molecular docking; Phaedranassa
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MDPI and ACS Style

Moreno, R.; Tallini, L.R.; Salazar, C.; Osorio, E.H.; Montero, E.; Bastida, J.; Oleas, N.H.; Acosta León, K. Chemical Profiling and Cholinesterase Inhibitory Activity of Five Phaedranassa Herb. (Amaryllidaceae) Species from Ecuador. Molecules 2020, 25, 2092.

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