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Cholinesterase inhibitory, anti-amyloidogenic and neuroprotective effect of the medicinal plant Grewia tiliaefolia – An in vitro and in silico study

Context:Grewia tiliaefolia Vahl. (Tiliaceae) is a sub-tropical plant used as an indigenous medicine in India. However, its efficacy has not been evaluated against Alzheimer’s disease. Objectives: The objective of this study is to evaluate cholinesterase inhibitory, anti-aggregation and neuroprotecti...

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Autores principales: Sheeja Malar, Dicson, Beema Shafreen, Rajamohamed, Karutha Pandian, Shunmugiah, Pandima Devi, Kasi
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Taylor & Francis 2016
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6130737/
https://www.ncbi.nlm.nih.gov/pubmed/27931177
http://dx.doi.org/10.1080/13880209.2016.1241811
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author Sheeja Malar, Dicson
Beema Shafreen, Rajamohamed
Karutha Pandian, Shunmugiah
Pandima Devi, Kasi
author_facet Sheeja Malar, Dicson
Beema Shafreen, Rajamohamed
Karutha Pandian, Shunmugiah
Pandima Devi, Kasi
author_sort Sheeja Malar, Dicson
collection PubMed
description Context:Grewia tiliaefolia Vahl. (Tiliaceae) is a sub-tropical plant used as an indigenous medicine in India. However, its efficacy has not been evaluated against Alzheimer’s disease. Objectives: The objective of this study is to evaluate cholinesterase inhibitory, anti-aggregation and neuroprotective activity of G. tiliaefolia. Materials and method:Grewia tiliaefolia leaves were collected from Eastern Ghats region, India, and subjected to successive extraction (petroleum ether, chloroform, ethyl acetate, methanol and water). The extracts were subjected to in vitro antioxidant, anticholinesterase and anti-aggregation assays. The active methanol extract (MEGT) was separated using column chromatography. LC-MS analysis was done and the obtained compounds were docked against acetylcholinesterase (AChE) enzyme to identify the active component. Results: Antioxidant assays demonstrated that the MEGT showed significant free radical scavenging activity at the IC(50) value of 71.5 ± 1.12 μg/mL. MEGT also exhibited significant dual cholinesterase inhibition with IC(50) value of 64.26 ± 2.56 and 54 ± 0.7 μg/mL for acetyl and butyrylcholinesterase (BChE), respectively. Also, MEGT showed significant anti-aggregation activity by preventing the oligomerization of Aβ(25–35). Further, MEGT increased the viability of Neuro2a cells up to 95% against Aβ(25-35) neurotoxicity. LC-MS analysis revealed the presence of 16 compounds including vitexin, ellagic acid, isovitexin, etc. In silico analysis revealed that vitexin binds effectively with AChE through strong hydrogen bonding. These results were further confirmed by evaluating the activity of vitexin in vitro, which showed dual cholinesterase inhibition with IC(50) value of 15.21 ± 0.41 and 19.75 ± 0.16 μM for acetyl and butyrlcholinesterase, respectively. Discussion and conclusion:Grewia tiliaefolia can be considered as a promising therapeutic agent for the treatment of AD.
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spelling pubmed-61307372018-09-27 Cholinesterase inhibitory, anti-amyloidogenic and neuroprotective effect of the medicinal plant Grewia tiliaefolia – An in vitro and in silico study Sheeja Malar, Dicson Beema Shafreen, Rajamohamed Karutha Pandian, Shunmugiah Pandima Devi, Kasi Pharm Biol Original Article Context:Grewia tiliaefolia Vahl. (Tiliaceae) is a sub-tropical plant used as an indigenous medicine in India. However, its efficacy has not been evaluated against Alzheimer’s disease. Objectives: The objective of this study is to evaluate cholinesterase inhibitory, anti-aggregation and neuroprotective activity of G. tiliaefolia. Materials and method:Grewia tiliaefolia leaves were collected from Eastern Ghats region, India, and subjected to successive extraction (petroleum ether, chloroform, ethyl acetate, methanol and water). The extracts were subjected to in vitro antioxidant, anticholinesterase and anti-aggregation assays. The active methanol extract (MEGT) was separated using column chromatography. LC-MS analysis was done and the obtained compounds were docked against acetylcholinesterase (AChE) enzyme to identify the active component. Results: Antioxidant assays demonstrated that the MEGT showed significant free radical scavenging activity at the IC(50) value of 71.5 ± 1.12 μg/mL. MEGT also exhibited significant dual cholinesterase inhibition with IC(50) value of 64.26 ± 2.56 and 54 ± 0.7 μg/mL for acetyl and butyrylcholinesterase (BChE), respectively. Also, MEGT showed significant anti-aggregation activity by preventing the oligomerization of Aβ(25–35). Further, MEGT increased the viability of Neuro2a cells up to 95% against Aβ(25-35) neurotoxicity. LC-MS analysis revealed the presence of 16 compounds including vitexin, ellagic acid, isovitexin, etc. In silico analysis revealed that vitexin binds effectively with AChE through strong hydrogen bonding. These results were further confirmed by evaluating the activity of vitexin in vitro, which showed dual cholinesterase inhibition with IC(50) value of 15.21 ± 0.41 and 19.75 ± 0.16 μM for acetyl and butyrlcholinesterase, respectively. Discussion and conclusion:Grewia tiliaefolia can be considered as a promising therapeutic agent for the treatment of AD. Taylor & Francis 2016-12-08 /pmc/articles/PMC6130737/ /pubmed/27931177 http://dx.doi.org/10.1080/13880209.2016.1241811 Text en © 2016 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. http://creativecommons.org/licenses/by/4.0/ This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Original Article
Sheeja Malar, Dicson
Beema Shafreen, Rajamohamed
Karutha Pandian, Shunmugiah
Pandima Devi, Kasi
Cholinesterase inhibitory, anti-amyloidogenic and neuroprotective effect of the medicinal plant Grewia tiliaefolia – An in vitro and in silico study
title Cholinesterase inhibitory, anti-amyloidogenic and neuroprotective effect of the medicinal plant Grewia tiliaefolia – An in vitro and in silico study
title_full Cholinesterase inhibitory, anti-amyloidogenic and neuroprotective effect of the medicinal plant Grewia tiliaefolia – An in vitro and in silico study
title_fullStr Cholinesterase inhibitory, anti-amyloidogenic and neuroprotective effect of the medicinal plant Grewia tiliaefolia – An in vitro and in silico study
title_full_unstemmed Cholinesterase inhibitory, anti-amyloidogenic and neuroprotective effect of the medicinal plant Grewia tiliaefolia – An in vitro and in silico study
title_short Cholinesterase inhibitory, anti-amyloidogenic and neuroprotective effect of the medicinal plant Grewia tiliaefolia – An in vitro and in silico study
title_sort cholinesterase inhibitory, anti-amyloidogenic and neuroprotective effect of the medicinal plant grewia tiliaefolia – an in vitro and in silico study
topic Original Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6130737/
https://www.ncbi.nlm.nih.gov/pubmed/27931177
http://dx.doi.org/10.1080/13880209.2016.1241811
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