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Bioorg Med Chem Lett. 2014 Jul 15;24(14):3108-12. doi: 10.1016/j.bmcl.2014.05.008. Epub 2014 May 13.

Naturally occurring polyphenolic inhibitors of amyloid beta aggregation.

Author information

1
CSIRO Materials Science and Engineering, 343 Royal Parade, Parkville, Victoria 3052, Australia. Electronic address: quentin.churches@csiro.au.
2
CSIRO Materials Science and Engineering, 343 Royal Parade, Parkville, Victoria 3052, Australia.
3
CSIRO Materials Science and Engineering, Bag 10, Clayton South, Victoria 3169, Australia.
4
CSIRO Materials Science and Engineering, Bag 10, Clayton South, Victoria 3169, Australia; School of Chemical and Physical Sciences, Flinders University, Adelaide, SA 5042, Australia.

Abstract

Alzheimer's disease is the most common neurodegenerative disease and is one of the main causes of death in developed countries. Consumption of foods rich in polyphenolics is strongly correlated with reduced incidence of Alzheimer's disease. Our study has investigated the biological activity of previously untested polyphenolic compounds in preventing amyloid β aggregation. The anti-aggregatory potential of these compounds was assessed using the Thioflavin-T assay, transmission electron microscopy, dynamic light scattering and size exclusion chromatography. Two structurally related compounds, luteolin and transilitin were identified as potent inhibitors of Aβ fibril formation. Computational docking studies with an X-ray derived oligomeric structure offer a rationale for the inhibitory activity observed and may facilitate development of improved inhibitors of Aβ aggregation and toxicity.

KEYWORDS:

Amyloid; Amyloid-beta peptide; Flavonoid; Flavonol; Isoflavone; Polyphenol

PMID:
24878198
DOI:
10.1016/j.bmcl.2014.05.008
[Indexed for MEDLINE]

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