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- Title
Discovery of Natural Inhibitors of Cholinesterases from Hydrangea : In Vitro and In Silico Approaches.
- Authors
Hwang, Jayeong; Youn, Kumju; Lim, Gyutae; Lee, Jinhyuk; Kim, Dong Hyun; Jun, Mira
- 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.
- Subjects
ACETYLCHOLINESTERASE; ALZHEIMER'S disease; BENZOPYRANS; BINDING sites; CARRIER proteins; CHOLINESTERASE inhibitors; MEDICINAL plants; NATURAL foods; PLANT extracts; IN vitro studies; MOLECULAR docking; PHARMACODYNAMICS
- Publication
Nutrients, 2021, Vol 13, Issue 1, p254
- ISSN
2072-6643
- Publication type
Article
- DOI
10.3390/nu13010254