Repositorio
Institucional

Hormazabal, Emilio

Moraga-Nicolas, Felipe#Jara, Claudia#Godoy, Ricardo#Iturriaga-Vasquez, Patricio#Venthur, Herbert#Quiroz, Andres#Becerra, Jose#Mutis, Ana

Rhodolirium andicola: a new renewable source of alkaloids with acetylcholinesterase inhibitory activity, a study from nature to molecular docking

SOC BRASILEIRA FARMACOGNOSIA

REVISTA BRASILEIRA DE FARMACOGNOSIA-BRAZILIAN JOURNAL OF PHARMACOGNOSY

en

Acetylcholinesterase is an important target for control of neurodegenerative diseases causing cholinergic signaling deficit. Traditionally, galanthamine has been used as an Amaryllidaceae-derived acetylcholinesterase inhibitor, although new Amaryllidaceae plants could serve as source for better acetylcholinesterase inhibitors. Therefore, the objective of this study was to characterize the alkaloid composition from bulbs of Rhodolirium andicola (Poepp.) Traub, a native Chilean Amaryllidaceae specie, and assess their inhibitory activity on acetylcholinesterase by in vitro and in silico methodologies. Alkaloidal extracts from R. andicola exhibited an inhibitory activity with IC50 values between 11.25 +/- 0.04 and 57.78 +/- 1.92 mu g/ml that included isolated alkaloid, galanthamine (2.3 +/- 0.18 mu g/ml), Additionally, 12 alkaloids were detected using gas chromatography-mass spectrometry and identified by comparing their mass fragmentation patterns with literature and database NIST vs.2.0. To better understand the bioactivity of isolated compounds and alkaloidal extracts against acetylcholinesterase, a molecular docking approach was performed. Results suggested that alkaloids such as lycoramine, norpluvine diacetate and 6 alpha-deoxy-tazettine expand the list of potential acetylcholinesterase inhibitors to not only galanthamine. The role of R. andicola as a source for acetylcholinesterase inhibitors is further discussed in this study. (C) 2018 Sociedade Brasileira de Farmacognosia. Published by Elsevier Editora Ltda. This is an open access article under the CC BY-NC-ND license.

Artículo original

The authors would like to acknowledge CONICYT scholarship No. 21140301 and project DIUFRO DI16-2007. Support for this research at Laboratory of Ecologia Quimica, Universidad de La Frontera, Chile, and FONDECYT No. 11140668. We are grateful to Dra. Gabriela Feresin, Dr. Alejandro Tapia and Dr. Beier' Aguero from Instituto de Biotecnologia, de la Universidad de San Juan, Argentina, and Dra. Isabel Bermudez professor in Neuropharmacology from Department of Biological and Medical Sciences - Faculty of Health and Life Sciences, Oxford Brookes University. Finally, we would like to thank the Center of Excellence in Modelling and Scientific Computing (CEMCC) of Universidad de La Frontera for its valuable help during molecular simulations.

Los autores agradecen la beca CONICYT n.° 21140301 y el proyecto DIUFRO DI16-2007. El apoyo para esta investigación del Laboratorio de Ecología Química de la Universidad de La Frontera, Chile, y el FONDECYT n.° 11140668. Agradecemos a la Dra. Gabriela Feresin, al Dr. Alejandro Tapia y al Dr. Beier' Aguero del Instituto de Biotecnología de la Universidad de San Juan, Argentina, y a la Dra. Isabel Bermúdez, profesora de Neurofarmacología del Departamento de Ciencias Biológicas y Médicas de la Facultad de Ciencias de la Salud y de la Vida de la Universidad Oxford Brookes. Finalmente, agradecemos al Centro de Excelencia en Modelamiento y Computación Científica (CEMCC) de la Universidad de La Frontera por su valiosa ayuda durante las simulaciones moleculares.

10.1016/j.bjp.2017.11.009

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Amaryllidaceae# Alkaloids# Acetylcholinesterase inhibitors# Molecular docking

http://dx.doi.org/10.1016/j.bjp.2017.11.009

Chemistry, Medicinal# Pharmacology & Pharmacy

Amarilidáceas# Alcaloides# Inhibidores de la acetilcolinesterasa# acoplamiento molecular

Farmacología y Farmacia

Química Orgánica

Botánica

WOS:000426442500006

<i>Rhodolirium andicola</i>: a new renewable source of alkaloids with acetylcholinesterase inhibitory activity, a study from nature to molecular docking

Artículo original

version publicada

SOC BRASILEIRA FARMACOGNOSIA

REVISTA BRASILEIRA DE FARMACOGNOSIA-BRAZILIAN JOURNAL OF PHARMACOGNOSY

Química Medicinal# Farmacología y farmacia

0102-695X

en

ANID CONICYT 21140301#UFRO DIUFRO DI16-2007ANID FONDECYT 11140668

ANID CONICYT 21140301

UFRO, Laboratory of Ecologia Quimica

ANID FONDECYT 11140668

UFRO DI16-2007

The authors would like to acknowledge CONICYT scholarship No. 21140301 and project DIUFRO DI16-2007. Support for this research at Laboratory of Ecologia Quimica, Universidad de La Frontera, Chile, and FONDECYT No. 11140668. We are grateful to Dra. Gabriela Feresin, Dr. Alejandro Tapia and Dr. Beier' Aguero from Instituto de Biotecnologia, de la Universidad de San Juan, Argentina, and Dra. Isabel Bermudez professor in Neuropharmacology from Department of Biological and Medical Sciences - Faculty of Health and Life Sciences, Oxford Brookes University. Finally, we would like to thank the Center of Excellence in Modelling and Scientific Computing (CEMCC) of Universidad de La Frontera for its valuable help during molecular simulations.

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CC BY-NC-ND 4.0