Cargando…

In vitro anti-acetylcholinesterase activity of an aqueous extract of Unicaria tomentosa and in silico study of its active constituents

Depletion of acetylcholine in the central nervous system (CNS) is responsible for memory loss and cognition deficit. Enzyme acetylcholinesterase (AChE) is responsible for destruction of acetylcholine (Ach) in the brain. Many herbal plant extracts have been investigated for their potential use in the...

Descripción completa

Detalles Bibliográficos
Autores principales: Chowdhury, Suman, Shivani, Kumar, Suresh
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Biomedical Informatics 2016
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5267953/
https://www.ncbi.nlm.nih.gov/pubmed/28149044
http://dx.doi.org/10.6026/97320630012112
_version_ 1782500725965717504
author Chowdhury, Suman
Shivani,
Kumar, Suresh
author_facet Chowdhury, Suman
Shivani,
Kumar, Suresh
author_sort Chowdhury, Suman
collection PubMed
description Depletion of acetylcholine in the central nervous system (CNS) is responsible for memory loss and cognition deficit. Enzyme acetylcholinesterase (AChE) is responsible for destruction of acetylcholine (Ach) in the brain. Many herbal plant extracts have been investigated for their potential use in the treatment of Alzheimer’s disease (AD) by inhibiting AChE and upregulating the levels of Ach. The current study investigated the anti-acetylcholinesterase (AChE) activity of an aqueous extract of Unicaria tomentosa bark which has not been reported so far in the literature. The in vitro study of an aqueous extract of U. tomentosa showed maximum inhibition of 76.2±0.002 % at 0.4mg/ml of final concentration with an IC50 = 0.112 mg/ml. The mechanism of inhibition was elucidated by kinetic study which showed mixed type of inhibition, this might be due to the presence of various phytoconstituents such as oxindole alkaloids present in an aqueous extract. Based on molecular structure of phytoconstituents obtained from U. tomentosa known from the relevant literature, in-silico molecular docking study was performed against AChE protein to validate the results.
format Online
Article
Text
id pubmed-5267953
institution National Center for Biotechnology Information
language English
publishDate 2016
publisher Biomedical Informatics
record_format MEDLINE/PubMed
spelling pubmed-52679532017-02-01 In vitro anti-acetylcholinesterase activity of an aqueous extract of Unicaria tomentosa and in silico study of its active constituents Chowdhury, Suman Shivani, Kumar, Suresh Bioinformation Hypothesis Depletion of acetylcholine in the central nervous system (CNS) is responsible for memory loss and cognition deficit. Enzyme acetylcholinesterase (AChE) is responsible for destruction of acetylcholine (Ach) in the brain. Many herbal plant extracts have been investigated for their potential use in the treatment of Alzheimer’s disease (AD) by inhibiting AChE and upregulating the levels of Ach. The current study investigated the anti-acetylcholinesterase (AChE) activity of an aqueous extract of Unicaria tomentosa bark which has not been reported so far in the literature. The in vitro study of an aqueous extract of U. tomentosa showed maximum inhibition of 76.2±0.002 % at 0.4mg/ml of final concentration with an IC50 = 0.112 mg/ml. The mechanism of inhibition was elucidated by kinetic study which showed mixed type of inhibition, this might be due to the presence of various phytoconstituents such as oxindole alkaloids present in an aqueous extract. Based on molecular structure of phytoconstituents obtained from U. tomentosa known from the relevant literature, in-silico molecular docking study was performed against AChE protein to validate the results. Biomedical Informatics 2016-06-15 /pmc/articles/PMC5267953/ /pubmed/28149044 http://dx.doi.org/10.6026/97320630012112 Text en © 2016 Biomedical Informatics This is an Open Access article which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly credited. This is distributed under the terms of the Creative Commons Attribution License.
spellingShingle Hypothesis
Chowdhury, Suman
Shivani,
Kumar, Suresh
In vitro anti-acetylcholinesterase activity of an aqueous extract of Unicaria tomentosa and in silico study of its active constituents
title In vitro anti-acetylcholinesterase activity of an aqueous extract of Unicaria tomentosa and in silico study of its active constituents
title_full In vitro anti-acetylcholinesterase activity of an aqueous extract of Unicaria tomentosa and in silico study of its active constituents
title_fullStr In vitro anti-acetylcholinesterase activity of an aqueous extract of Unicaria tomentosa and in silico study of its active constituents
title_full_unstemmed In vitro anti-acetylcholinesterase activity of an aqueous extract of Unicaria tomentosa and in silico study of its active constituents
title_short In vitro anti-acetylcholinesterase activity of an aqueous extract of Unicaria tomentosa and in silico study of its active constituents
title_sort in vitro anti-acetylcholinesterase activity of an aqueous extract of unicaria tomentosa and in silico study of its active constituents
topic Hypothesis
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5267953/
https://www.ncbi.nlm.nih.gov/pubmed/28149044
http://dx.doi.org/10.6026/97320630012112
work_keys_str_mv AT chowdhurysuman invitroantiacetylcholinesteraseactivityofanaqueousextractofunicariatomentosaandinsilicostudyofitsactiveconstituents
AT shivani invitroantiacetylcholinesteraseactivityofanaqueousextractofunicariatomentosaandinsilicostudyofitsactiveconstituents
AT kumarsuresh invitroantiacetylcholinesteraseactivityofanaqueousextractofunicariatomentosaandinsilicostudyofitsactiveconstituents