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Review
. 2021 Feb 25;11(3):350.
doi: 10.3390/biom11030350.

Acetylcholinesterase Inhibitory Potential of Various Sesquiterpene Analogues for Alzheimer's Disease Therapy

Ashwani Arya  1 , Rubal Chahal  1 , Rekha Rao  2 , Md Habibur Rahman  3   4 , Deepak Kaushik  1 , Muhammad Furqan Akhtar  5 , Ammara Saleem  6 , Shaden M A Khalifa  7 , Hesham R El-Seedi  8   9   10 , Mohamed Kamel  11 , Ghadeer M Albadrani  12 , Mohamed M Abdel-Daim  13 , Vineet Mittal  1
Affiliations
Review

V体育官网 - Acetylcholinesterase Inhibitory Potential of Various Sesquiterpene Analogues for Alzheimer's Disease Therapy

Ashwani Arya et al. Biomolecules. .

Abstract

Alzheimer's disease (AD) is a gradually growing irreversible illness of the brain that almost affects every fifth person (aged > 80 years) in the world. World Health Organization (WHO) also revealed that the prevalence of this disease will enhance (upto double) significantly upto 2030. The poor cholinergic transmission at the synapse is considered to be one of the main reasons behind the progression and occurrence of this disorder. Natural inhibitors of acetylcholine (ACh) such as galanthamine and rivastigmine are used commercially in the treatmentof AD. The biomolecules such assesquiterpenes, possess a great structural diversity and are responsible for a plethora of pharmacological properties. The potential of various sesquiterpenes as anticholinesterase has been reviewed in this article. For this purpose, the various databases, mainly PubMed, Scopus, and Web of Science were investigatedwith different keywords such as "sesquiterpenes+acetylcholinesterase" and "sesquiterpenes+cholinesterase+inhibitors" in the surveyed time frame (2010-2020). A vast literature was evident in the last decade, which affirms the potential of various sesquiterpenes in the improvement of cholinergic transmission by inhibiting the AChE. After data analysis, it was found that 12 compounds out of a total of 58 sesquiterpenes were reported to possess IC50 < 9μM and can be considered as potential candidates for the improvement of learning and memory. Sesquiterpene is an important category of terpenoids, found to possess a large spectrum of biological activities. The outcome of the review clearly states that sesquiterpenes (such as amberboin, lipidiol,etc) from herbs could offer fresh, functional compounds for possible prevention and treatment of AD VSports手机版. .

Keywords: Alzheimer’s disease; acetylcholinesterase; cognition; coumarins; lactones; neurodegeneration; phytochemicals. V体育安卓版.

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"V体育2025版" Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Acetylcholine (Ach) transmission through synapse (cholinergic transmission) and action of acetylcholinesterase (AChE) on acetylcholine. ACh: acetylcholine; AChE: acetylcholinesterase; PAS: peripheral anionic site; CAS:catalytic active site; TRY: tryptophan; SER: serine; HIS: histidine; GLU: glutamate.
Figure 2
Figure 2
Various sesquiterpenoids moieties with AChE/BChE inhibitory potential.
Figure 2
Figure 2
Various sesquiterpenoids moieties with AChE/BChE inhibitory potential.
Figure 3
Figure 3
Sesquiterpene lactones/their derivatives for AChE inhibition.
Figure 4
Figure 4
Structure of miscellaneous sesquiterpenes found effective against acetylcholinesterase.
Figure 5
Figure 5
Percentage of various categories of sesquiterpenes with AChE inhibitory potential.
See this image and copyright information in PMC

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