Abstract：
BACKGROUND:The major hallmark of Alzheimer's disease (AD) is the formation of amyloid aggregates, which are formed due to improper folding of proteins leading to the aggregation of amyloid beta (Aβ) 42 peptide. Inhibition of Aβ 42 aggregation using a drug such as carbenoxolone (Cbx), which has already been stated as neuroprotective, appears to be an effective approach against AD. OBJECTIVE:The present study was designed to investigate the anti-fibrillation activity of Cbx against the Aβ 42 aggregation. METHODS:The aggregation of Aβ 42 peptide was observed by performing in-vitro studies and the propensity of aggregation of Aβ 42 peptide was evaluated by the prediction of binding sites and amyloidogenic regions. The binding of Cbx in these binding sites was predicted by computational studies. RESULTS:Thioflavin-T (Th-T assay), congo red assay and circular dichroism (CD) analysis suggested significant inhibition of Aβ 42 aggregation by Cbx. The propensity of aggregation of Aβ 42 peptide was evaluated by the prediction of binding sites and amyloidogenic regions. The mechanism of anti-fibrillation activity of Cbx was elucidated by molecular docking and simulation studies and has been predicted to interact with amyloidogenic residues of Aβ 42 peptides as well as fibrils. Cbx also interacts with residues involved in the stabilization of the oligomeric structure. CONCLUSION:These results project Cbx as a suitable candidate for the inhibition of Aβ 42 aggregation and the therapeutic potential of Cbx against AD can further be studied using in-vivo experiments.
journal_name
Neurochem Intjournal_title
Neurochemistry internationalauthors
Sharma S,Nehru B,Saini Adoi
10.1016/j.neuint.2017.06.011subject
Has Abstractpub_date
2017-09-01 00:00:00pages
481-493eissn
0197-0186issn
1872-9754pii
S0197-0186(17)30146-8journal_volume
108pub_type
杂志文章abstract：:Astroglial cells have a variety of roles in the central nervous system (CNS), providing a homeostasis for the proper functioning of neuronal cells. The classical view concerning the supportive role of astroglia towards associated neurons has to be extended. A great number of new evidences suggest that astrocytes inter...
journal_title：Neurochemistry international
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journal_title：Neurochemistry international
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journal_title：Neurochemistry international
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journal_title：Neurochemistry international
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doi：10.1016/j.neuint.2008.12.003
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pub_type： 杂志文章,评审
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journal_title：Neurochemistry international
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journal_title：Neurochemistry international
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journal_title：Neurochemistry international
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