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Flavanone Glycosides as Acetylcholinesterase Inhibitors: Computational and Experimental Evidence

Acetylcholinesterase hydrolyzes the neurotransmitter called acetylcholine and is crucially involved in the regulation of neurotransmission. One of the observable facts in the neurodegenerative disorders like Alzheimer's disease is the decrease in the level of acetylcholine. Available drugs that...

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Autores principales: Remya, C., Dileep, K. V., Tintu, I., Variyar, E. J., Sadasivan, C.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Medknow Publications & Media Pvt Ltd 2014
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4293693/
https://www.ncbi.nlm.nih.gov/pubmed/25593395
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author Remya, C.
Dileep, K. V.
Tintu, I.
Variyar, E. J.
Sadasivan, C.
author_facet Remya, C.
Dileep, K. V.
Tintu, I.
Variyar, E. J.
Sadasivan, C.
author_sort Remya, C.
collection PubMed
description Acetylcholinesterase hydrolyzes the neurotransmitter called acetylcholine and is crucially involved in the regulation of neurotransmission. One of the observable facts in the neurodegenerative disorders like Alzheimer's disease is the decrease in the level of acetylcholine. Available drugs that are used for the treatment of Alzheimer's disease are primarily acetylcholinesterase inhibitors with multiple activities. They maintain the level of acetylcholine in the brain by inhibiting the acetylcholinesterase function. Hence acetylcholinesterase inhibitors can be used as lead compounds for the development of drugs against AD. In the present study, the binding potential of four flavanone glycosides such as naringin, hesperidin, poncirin and sakuranin against acetylcholinesterase was analysed by using the method of molecular modeling and docking. The activity of the top scored compound, naringin was further investigated by enzyme inhibition studies and its inhibitory concentration (IC(50)) towards acetylcholinesterase was also determined.
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spelling pubmed-42936932015-01-15 Flavanone Glycosides as Acetylcholinesterase Inhibitors: Computational and Experimental Evidence Remya, C. Dileep, K. V. Tintu, I. Variyar, E. J. Sadasivan, C. Indian J Pharm Sci Short Communication Acetylcholinesterase hydrolyzes the neurotransmitter called acetylcholine and is crucially involved in the regulation of neurotransmission. One of the observable facts in the neurodegenerative disorders like Alzheimer's disease is the decrease in the level of acetylcholine. Available drugs that are used for the treatment of Alzheimer's disease are primarily acetylcholinesterase inhibitors with multiple activities. They maintain the level of acetylcholine in the brain by inhibiting the acetylcholinesterase function. Hence acetylcholinesterase inhibitors can be used as lead compounds for the development of drugs against AD. In the present study, the binding potential of four flavanone glycosides such as naringin, hesperidin, poncirin and sakuranin against acetylcholinesterase was analysed by using the method of molecular modeling and docking. The activity of the top scored compound, naringin was further investigated by enzyme inhibition studies and its inhibitory concentration (IC(50)) towards acetylcholinesterase was also determined. Medknow Publications & Media Pvt Ltd 2014 /pmc/articles/PMC4293693/ /pubmed/25593395 Text en Copyright: © Indian Journal of Pharmaceutical Sciences http://creativecommons.org/licenses/by-nc-sa/3.0 This is an open-access article distributed under the terms of the Creative Commons Attribution-Noncommercial-Share Alike 3.0 Unported, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Short Communication
Remya, C.
Dileep, K. V.
Tintu, I.
Variyar, E. J.
Sadasivan, C.
Flavanone Glycosides as Acetylcholinesterase Inhibitors: Computational and Experimental Evidence
title Flavanone Glycosides as Acetylcholinesterase Inhibitors: Computational and Experimental Evidence
title_full Flavanone Glycosides as Acetylcholinesterase Inhibitors: Computational and Experimental Evidence
title_fullStr Flavanone Glycosides as Acetylcholinesterase Inhibitors: Computational and Experimental Evidence
title_full_unstemmed Flavanone Glycosides as Acetylcholinesterase Inhibitors: Computational and Experimental Evidence
title_short Flavanone Glycosides as Acetylcholinesterase Inhibitors: Computational and Experimental Evidence
title_sort flavanone glycosides as acetylcholinesterase inhibitors: computational and experimental evidence
topic Short Communication
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4293693/
https://www.ncbi.nlm.nih.gov/pubmed/25593395
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