Bioorganic & Medicinal Chemistry Letters

2013 
abstract Alzheimer’s disease is the most common neurodegenerative disease and is one of the main causes ofdeath in developed countries. Consumption of foods rich in polyphenolics is strongly correlated withreduced incidence of Alzheimer’s disease. Our study has investigated the biological activity of previouslyuntested polyphenolic compounds in preventing amyloid b aggregation. The anti-aggregatory potential ofthese compounds was assessed using the Thioflavin-T assay, transmission electron microscopy, dynamiclight scattering and size exclusion chromatography. Two structurally related compounds, luteolin andtransilitin were identified as potent inhibitors of Ab fibril formation. Computational docking studies withan X-ray derived oligomeric structure offer a rationale for the inhibitory activity observed and may facil-itate development of improved inhibitors of Ab aggregation and toxicity.Crown Copyright 2014 Published by Elsevier Ltd. All rights reserved. Alzheimer’s Disease (AD) is the most common form of dementiaaffecting the elderly population and is characterized by gradualmemory loss, behavioral change and by the formation of cerebralplaques formed by deposition of amyloid-beta (Ab) protein. Theamyloid cascade hypothesis is the most widely accepted explana-tion of the overall disease pathology.
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