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The National Agricultural Library is one of four national libraries of the United States, with locations in Beltsville, Maryland and Washington, D.C. It houses one of the world's largest and most accessible agricultural information collections and serves as the nexus for a national network of state land-grant and U.S. Department of Agriculture field libraries. In fiscal year 2011 (Oct 2010 through Sept 2011) NAL delivered more than 100 million direct customer service transactions.

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Journal Article

Journal Article

Dual inhibition of BACE1 and Aβ aggregation by β-ecdysone: Application of a phytoecdysteroid scaffold in Alzheimer’s disease therapeutics  [2017]

Chakraborty, Sandipan; Soumalee Basu;

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Current medications for the complex neurological disorder, Alzheimer’s disease (AD), can neither stop disease progression nor revert back disease pathogenesis. The present study demonstrates the applicability of a phytoecdysteroid, β-ecdysone, as a multi-potent agent in AD therapeutics. β-ecdysone strongly binds to the active site cavity of BACE1 with calculated dissociation constant of 1.75±0.1μM. Steady-state and time-resolved fluorescence spectroscopy reveal that binding of β-ecdysone induces conformational transition of the protein from open to closed form thereby blocking substrate binding. Even 500nM of the compound completely blocks the enzyme activity. Furthermore, β-ecdysone strongly inhibits Aβ aggregation, evident from ANS and ThT binding assay. Co-incubation of equimolar peptide and β-ecdysone completely inhibits Aβ fibril formation which is further complemented by the AFM study. Low systemic toxicity of β-ecdysone further extends the applicability of the compound as functional food and dietary supplement for disease management.
From the journal
International journal of biological macromolecules
ISSN : 0141-8130

Bibliographic information

Language:
English
Type:
Journal Article
In AGRIS since:
2017
Volume:
95
Start Page:
281
End Page:
287
Publisher:
Elsevier B.V.
All titles:
"Dual inhibition of BACE1 and Aβ aggregation by β-ecdysone: Application of a phytoecdysteroid scaffold in Alzheimer’s disease therapeutics"@eng
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Bibliographic information

Language:
English
Type:
Journal Article
In AGRIS since:
2017
Volume:
95
Start Page:
281
End Page:
287
Publisher:
Elsevier B.V.
All titles:
"Dual inhibition of BACE1 and Aβ aggregation by β-ecdysone: Application of a phytoecdysteroid scaffold in Alzheimer’s disease therapeutics"@eng