Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 26, Issue 15, Pages 3785-3792Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2016.05.046
Keywords
Myristica cinnamomea King; Myristicaceae; Acylphenols; Dimeric acylphenols; Malabaricone E; Acetylcholinesterase enzyme; Butyrylcholinesterase enzyme
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Funding
- University of Malaya Research Grant [RP001-2012A/B]
- Centre National de la Recherche Scientifique (CNRS) [57-02-03-1007]
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A new acylphenol, malabaricone E (1) together with the known malabaricones A-C (2-4), maingayones A and B (5 and 6) and maingayic acid B (7) were isolated from the ethyl acetate extract of the fruits of Myristica cinnamomea King. Their structures were determined by 1D and 2D NMR techniques and LCMS-IT-TOF analysis. Compounds 3 (1.84 +/- 0.19 and 1.76 +/- 0.21 mu M, respectively) and 4 (1.94 +/- 0.27 and 2.80 +/- 0.49 mu M, respectively) were identified as dual inhibitors, with almost equal acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes inhibiting potentials. The Lineweaver-Burk plots of compounds 3 and 4 indicated that they were mixed-mode inhibitors. Based on the molecular docking studies, compounds 3 and 4 interacted with the peripheral anionic site (PAS), the catalytic triad and the oxyanion hole of the AChE. As for the BChE, while compound 3 interacted with the PAS, the catalytic triad and the oxyanion hole, compound 4 only interacted with the catalytic triad and the oxyanion hole. (C) 2016 Elsevier Ltd. All rights reserved.
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