Chemical Profiling and Cholinesterase Inhibitory Activity of Five <i>Phaedranassa</i> Herb. (Amaryllidaceae) Species from Ecuador
Raúl Moreno,
Luciana R. Tallini,
Cristina Salazar,
Edison H. Osorio,
Evelin Montero,
Jaume Bastida,
Nora H. Oleas,
Karen Acosta León
Affiliations
Raúl Moreno
Group of Natural Products, Faculty of Pharmacy, University of Barcelona, Av. Joan XXIII, 27-31, 08028 Barcelona, Spain
Luciana R. Tallini
Group of Natural Products, Faculty of Pharmacy, University of Barcelona, Av. Joan XXIII, 27-31, 08028 Barcelona, Spain
Cristina Salazar
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
Edison H. Osorio
Facultad de Ciencias Naturales y Matemáticas, Universidad de Ibagué, Carrera 22 Calle 67, Ibagué 730001, Colombia
Evelin Montero
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
Jaume Bastida
Group of Natural Products, Faculty of Pharmacy, University of Barcelona, Av. Joan XXIII, 27-31, 08028 Barcelona, Spain
Nora H. Oleas
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
Karen Acosta León
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
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.
