Isolation and Characterisation of Acetylcholinesterase Inhibitors from Aquilaria subintegra for the Treatment of Alzheimer’s Disease (AD)

2014 ◽  
Vol 11 (2) ◽  
pp. 206-214 ◽  
Author(s):  
Hirbod Bahrani ◽  
Jamaludin Mohamad ◽  
Mohammadjavad Paydar ◽  
Hussin Rothan
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Acetylcholinesterase Inhibitors

Spirocyclohexadienones as an Uncommon Scaffold for Acetylcholinesterase Inhibitory Activity

2019 ◽  
Vol 15 (4) ◽  
pp. 373-382 ◽  
Author(s):  
Ralph C. Gomes ◽  
Renata P. Sakata ◽  
Wanda P. Almeida ◽  
Fernando Coelho
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Population Aging ◽  
Acetylcholinesterase Inhibitors ◽  
Acetylcholinesterase Activity ◽  
Docking Study ◽  
Biological Properties ◽  
Ache Inhibitor ◽  
Molecular Docking Study

Background: The most important cause of dementia affecting elderly people is the Alzheimer’s disease (AD). Patients affected by this progressive and neurodegenerative disease have severe memory and cognitive function impairments. Some medicines used for treating this disease in the early stages are based on inhibition of acetylcholinesterase. Population aging should contribute to increase the cases of patients suffering from Alzheimer's disease, thus requiring the development of new therapeutic entities for the treatment of this disease. Methods: The objective of this work is to identify new substances that have spatial structural similarity with donepezil, an efficient commercial drug used for the treatment of Alzheimer's disease, and to evaluate the capacity of inhibition of these new substances against the enzyme acetylcholinesterase. Results: Based on a previous results of our group, we prepared a set of 11 spirocyclohexadienones with different substitutions patterns in three steps and overall yield of up to 59%. These compounds were evaluated in vitro against acetylcholinesterase. We found that eight of them are able to inhibit the acetylcholinesterase activity, with IC50 values ranging from 0.12 to 12.67 µM. Molecular docking study indicated that the spirocyclohexadienone, 9e (IC50 = 0.12 µM), a mixedtype AChE inhibitor, showed a good interaction at active site of the enzyme, including the cationic (CAS) and the peripheral site (PAS). Conclusion: We described the first study aimed at investigating the biological properties of spirocyclohexadienones as acetylcholinesterase inhibitors. Thus, we have identified an inhibitor, which provided valuable insights for further studies aimed at the discovery of more potent acetylcholinesterase inhibitors.

Comprehensive review on Alzheimer's Disease: Pathophysiology and its Treatment

2021 ◽  
Vol 4 (3) ◽  
pp. 3-12
Author(s):  
Prativa Sadhu ◽  
◽  
Srijani Sen ◽  
Catherine Vanlalhriatpuii ◽  
◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Clinical Signs ◽  
Acetylcholinesterase Inhibitors ◽  
Neuron Activity ◽  
Aβ Peptides ◽  
Comprehensive Review ◽  
Thinking Ability ◽  
The Cost ◽  
Amyloid Cascade

Neurodegenerative disorders are marked by the loss of brain neuron activity, resulting in gradual cognitive impairment. The effects of neurodegenerative diseases are severe in terms of pathology and the cost of patient care. The aged, in general, are the most vulnerable. Alzheimer's disease (AD) is a brain ailment that causes cell degradation and is the leading cause of dementia, identified by a loss of thinking ability and independence in daily tasks. The amyloid cascade hypothesis, which attributes clinical signs/symptoms to an abundance of amyloid-beta (Aβ) peptides, enhanced deposition into amyloid plaques, and eventually neuronal destruction, is one theory for pathogenesis AD. The use of acetylcholinesterase inhibitors in AD treatment is based on their favorable effects on the disease's functional, cognitive and behavioral symptoms. However, their involvement in AD pathogenesis is uncertain. This comprehensive review will provide an overview of AD, including the pathophysiology, causes, treatments, and future treatment.

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