Rhodolirium andicola: a new renewable source of alkaloids with acetylcholinesterase inhibitory activity, a study from nature to molecular docking
ABSTRACT 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 µg/ml that included isolated alkaloid, galanthamine (2.3 ± 0.18 µg/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 6α-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.
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Sociedade Brasileira de Farmacognosia
2018
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oai:scielo:S0102-695X20180001000342018-03-20Rhodolirium andicola: a new renewable source of alkaloids with acetylcholinesterase inhibitory activity, a study from nature to molecular dockingMoraga-Nicolás,FelipeJara,ClaudiaGodoy,RicardoIturriaga-Vásquez,PatricioVenthur,HerbertQuiroz,AndrésBecerra,JoséMutis,AnaHormazábal,Emilio Amaryllidaceae Alkaloids Acetylcholinesterase inhibitors Molecular docking ABSTRACT 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 µg/ml that included isolated alkaloid, galanthamine (2.3 ± 0.18 µg/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 6α-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.info:eu-repo/semantics/openAccessSociedade Brasileira de FarmacognosiaRevista Brasileira de Farmacognosia v.28 n.1 20182018-01-01info:eu-repo/semantics/articletext/htmlhttp://old.scielo.br/scielo.php?script=sci_arttext&pid=S0102-695X2018000100034en10.1016/j.bjp.2017.11.009 |
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Moraga-Nicolás,Felipe Jara,Claudia Godoy,Ricardo Iturriaga-Vásquez,Patricio Venthur,Herbert Quiroz,Andrés Becerra,José Mutis,Ana Hormazábal,Emilio |
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Moraga-Nicolás,Felipe Jara,Claudia Godoy,Ricardo Iturriaga-Vásquez,Patricio Venthur,Herbert Quiroz,Andrés Becerra,José Mutis,Ana Hormazábal,Emilio Rhodolirium andicola: a new renewable source of alkaloids with acetylcholinesterase inhibitory activity, a study from nature to molecular docking |
author_facet |
Moraga-Nicolás,Felipe Jara,Claudia Godoy,Ricardo Iturriaga-Vásquez,Patricio Venthur,Herbert Quiroz,Andrés Becerra,José Mutis,Ana Hormazábal,Emilio |
author_sort |
Moraga-Nicolás,Felipe |
title |
Rhodolirium andicola: a new renewable source of alkaloids with acetylcholinesterase inhibitory activity, a study from nature to molecular docking |
title_short |
Rhodolirium andicola: a new renewable source of alkaloids with acetylcholinesterase inhibitory activity, a study from nature to molecular docking |
title_full |
Rhodolirium andicola: a new renewable source of alkaloids with acetylcholinesterase inhibitory activity, a study from nature to molecular docking |
title_fullStr |
Rhodolirium andicola: a new renewable source of alkaloids with acetylcholinesterase inhibitory activity, a study from nature to molecular docking |
title_full_unstemmed |
Rhodolirium andicola: a new renewable source of alkaloids with acetylcholinesterase inhibitory activity, a study from nature to molecular docking |
title_sort |
rhodolirium andicola: a new renewable source of alkaloids with acetylcholinesterase inhibitory activity, a study from nature to molecular docking |
description |
ABSTRACT 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 µg/ml that included isolated alkaloid, galanthamine (2.3 ± 0.18 µg/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 6α-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. |
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Sociedade Brasileira de Farmacognosia |
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2018 |
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http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0102-695X2018000100034 |
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