Structure–activity relationship study of secondary metabolites from Mesua beccariana, Mesua ferrea and Mesua congestiflora for anti-cholinesterase activity

Our search for potential anti-acetylcholinesterase (AChE) inhibitors for treatment of Alzheimer’s disease has led to the discovery of two bioactive compounds, α-mangostin (11) and congestiflorone acetate (13). This discovery was achieved from a preliminary screening of the anti-AChE activity on the...

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Main Authors: Teh, Soek Sin, Cheng, Gwendoline Lian Ee, Mah, Siau Hui, Ahmad, Zuraini
Format: Article
Language:English
Published: Springer Verlag 2016
Subjects:
Online Access:http://psasir.upm.edu.my/id/eprint/53914/1/Structure%E2%80%93activity%20relationship%20study%20of%20secondary%20metabolites%20from%20Mesua%20beccariana.pdf
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author Teh, Soek Sin
Cheng, Gwendoline Lian Ee
Mah, Siau Hui
Ahmad, Zuraini
author_facet Teh, Soek Sin
Cheng, Gwendoline Lian Ee
Mah, Siau Hui
Ahmad, Zuraini
author_sort Teh, Soek Sin
collection UPM
description Our search for potential anti-acetylcholinesterase (AChE) inhibitors for treatment of Alzheimer’s disease has led to the discovery of two bioactive compounds, α-mangostin (11) and congestiflorone acetate (13). This discovery was achieved from a preliminary screening of the anti-AChE activity on the extracts of three Mesua species namely M. ferrea, M. beccariana and M. congestiflora using Ellman’s method. The pure metabolites, 1–12 which were isolated from the Mesua species, along with a synthetic derivative, compound 13 were then evaluated for their activities in order to identify the compounds that correspond to the enzyme inhibitory activities. Compounds 11 and 13 were found to give significant anti-AChE activities with IC50 values of 17.51 and 20.25 µM.
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spelling upm.eprints-539142018-02-21T03:52:13Z http://psasir.upm.edu.my/id/eprint/53914/ Structure–activity relationship study of secondary metabolites from Mesua beccariana, Mesua ferrea and Mesua congestiflora for anti-cholinesterase activity Teh, Soek Sin Cheng, Gwendoline Lian Ee Mah, Siau Hui Ahmad, Zuraini Our search for potential anti-acetylcholinesterase (AChE) inhibitors for treatment of Alzheimer’s disease has led to the discovery of two bioactive compounds, α-mangostin (11) and congestiflorone acetate (13). This discovery was achieved from a preliminary screening of the anti-AChE activity on the extracts of three Mesua species namely M. ferrea, M. beccariana and M. congestiflora using Ellman’s method. The pure metabolites, 1–12 which were isolated from the Mesua species, along with a synthetic derivative, compound 13 were then evaluated for their activities in order to identify the compounds that correspond to the enzyme inhibitory activities. Compounds 11 and 13 were found to give significant anti-AChE activities with IC50 values of 17.51 and 20.25 µM. Springer Verlag 2016 Article PeerReviewed text en http://psasir.upm.edu.my/id/eprint/53914/1/Structure%E2%80%93activity%20relationship%20study%20of%20secondary%20metabolites%20from%20Mesua%20beccariana.pdf Teh, Soek Sin and Cheng, Gwendoline Lian Ee and Mah, Siau Hui and Ahmad, Zuraini (2016) Structure–activity relationship study of secondary metabolites from Mesua beccariana, Mesua ferrea and Mesua congestiflora for anti-cholinesterase activity. Medicinal Chemistry Research, 25 (5). pp. 819-823. ISSN 1054-2523; ESSN: 1554-8120 https://link.springer.com/article/10.1007/s00044-016-1531-0 Anti-acetylcholinesterase; Mesua ferrea; Mesua beccariana; Mesua congestiflora; α-mangostin; Congestiflorone acetate 10.1007/s00044-016-1531-0
spellingShingle Anti-acetylcholinesterase; Mesua ferrea; Mesua beccariana; Mesua congestiflora; α-mangostin; Congestiflorone acetate
Teh, Soek Sin
Cheng, Gwendoline Lian Ee
Mah, Siau Hui
Ahmad, Zuraini
Structure–activity relationship study of secondary metabolites from Mesua beccariana, Mesua ferrea and Mesua congestiflora for anti-cholinesterase activity
title Structure–activity relationship study of secondary metabolites from Mesua beccariana, Mesua ferrea and Mesua congestiflora for anti-cholinesterase activity
title_full Structure–activity relationship study of secondary metabolites from Mesua beccariana, Mesua ferrea and Mesua congestiflora for anti-cholinesterase activity
title_fullStr Structure–activity relationship study of secondary metabolites from Mesua beccariana, Mesua ferrea and Mesua congestiflora for anti-cholinesterase activity
title_full_unstemmed Structure–activity relationship study of secondary metabolites from Mesua beccariana, Mesua ferrea and Mesua congestiflora for anti-cholinesterase activity
title_short Structure–activity relationship study of secondary metabolites from Mesua beccariana, Mesua ferrea and Mesua congestiflora for anti-cholinesterase activity
title_sort structure activity relationship study of secondary metabolites from mesua beccariana mesua ferrea and mesua congestiflora for anti cholinesterase activity
topic Anti-acetylcholinesterase; Mesua ferrea; Mesua beccariana; Mesua congestiflora; α-mangostin; Congestiflorone acetate
url http://psasir.upm.edu.my/id/eprint/53914/1/Structure%E2%80%93activity%20relationship%20study%20of%20secondary%20metabolites%20from%20Mesua%20beccariana.pdf
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