Discovery of natural inhibitors of cholinesterases from Hydrangea: in vitro and in silico approaches

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Title
Discovery of natural inhibitors of cholinesterases from Hydrangea: in vitro and in silico approaches
Author(s)
J Hwang; K Youn; Gyutae Lim; Jinhyuk Lee; D H Kim; M Jun
Bibliographic Citation
Nutrients, vol. 13, no. 1, pp. 254-254
Publication Year
2021
Abstract
Alzheimer's disease (AD) is a neurodegenerative disease conceptualized as a clinical-biological neurodegenerative construct where amyloid-beta pathophysiology is supposed to play a role. The loss of cognitive functions is mostly characterized by the rapid hydrolysis of acetylcholine by cholinesterases including acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Moreover, both enzymes are responsible for non-catalytic actions such as interacting with amyloid β peptide (Aβ) which further leads to promote senile plaque formation. In searching for a natural cholinesterase inhibitor, the present study focused on two isocoumarines from hydrangea, thunberginol C (TC) and hydrangenol 8-O-glucoside pentaacetate (HGP). Hydrangea-derived compounds were demonstrated to act as dual inhibitors of both AChE and BChE. Furthermore, the compounds exerted selective and non-competitive mode of inhibition via hydrophobic interaction with peripheral anionic site (PAS) of the enzymes. Overall results demonstrated that these natural hydrangea-derived compounds acted as selective dual inhibitors of AChE and BChE, which provides the possibility of potential source of new type of anti-cholinesterases with non-competitive binding property with PAS.
Keyword
Alzheimer’s disease (AD)CholinesteraseMolecular dockingThunberginol CHydrangenol 8-O-glucoside pentaacetate
ISSN
2072-6643
Publisher
MDPI
DOI
http://dx.doi.org/10.3390/nu13010254
Type
Article
Appears in Collections:
Division of Biomedical Research > Disease Target Structure Research Center > 1. Journal Articles
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