Natural cholinesterase inhibitors from Myristica cinnamomea king / Siti Mariam Abdul Wahab
A new acylphenol, malabaricone E (72) together with the known malabaricones A-C (1- 3), maingayones A and B (4 and 5) and maingayic acid B (69) 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...
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| Format: | Thesis |
| Published: |
2016
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| Online Access: | http://studentsrepo.um.edu.my/9665/1/Siti_Mariam_Abdul_Wahab.pdf http://studentsrepo.um.edu.my/9665/8/mariam.pdf http://studentsrepo.um.edu.my/9665/ |
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| Summary: | A new acylphenol, malabaricone E (72) together with the known malabaricones A-C (1-
3), maingayones A and B (4 and 5) and maingayic acid B (69) 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 2
(1.84 ± 0.19 and 1.76 ± 0.21 μM, respectively) and 3 (1.94 ± 0.27 and 2.80 ± 0.49 μM,
respectively) were identified as dual inhibitors, with almost equal acetylcholinesterase
enzyme (AChE) and butyrylcholinesterase enzyme (BChE) inhibiting potentials. The
Lineweaver-Burk plots of compounds 2 and 3 indicated that they were mixed-mode
inhibitors. Based on the molecular docking studies, compounds 2 and 3 interacted with
the peripheral anionic site (PAS), the catalytic triad and the oxyanion hole of the AChE.
As for the BChE, while compound 2 interacted with the PAS, the catalytic triad and the
oxyanion hole, compound 3 only interacted with the catalytic triad and the oxyanion
hole. |
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