The potential of naturally occurring polyphenols as nutraceuticals to prevent and/or treat Alzheimer's disease is studied. Five structurally related flavones and four tyrosols were tested in human amyloid-β peptide aggregation assays. The most promising compounds were two flavones, scutellarein and baicalein, and two tyrosols hydroxytyrosol and hydroxytyrosol acetate. These compounds caused a dose-dependent reduction of Aβ-peptide aggregation up to 90% for the flavones and 100% for the tyrosols, at concentrations of 83.3 μM and 33.3 mM, respectively. The IC value obtained for scutellarein was 22.5 μM, and was slightly higher for baicalein, 25.9 μM, while for hydroxytyrosol and hydroxytyrosol acetate they were 0.57 mM and 0.62 mM. Given these results, the compounds were selected to conduct assays with the animal model of Alzheimer's disease. The amyloid anti-aggregation ability of these polyphenols was demonstrated in aggregation assays in which 1 mM hydroxytyrosol reduced the amyloid plaques in the mutant strain CL2331 by 43%. The neuroprotective effect was evaluated in chemotaxis experiments carried out with transgenic strain CL2355 that expresses the human amyloid-β peptide in the neurons. The chemotaxis index was improved by 240% when the neuron-impaired animals were treated with 1 mM hydroxytyrosol. The results indicate that the four molecules would be viable candidates to develop nutraceuticals that interfere in amyloid-β peptide aggregation and, consequently, prevent and/or treat Alzheimer's disease.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1039/d1fo02147h | DOI Listing |
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!