Abstract
Silymarin, the seed extract of Silybium marianum, has preventive effects against Alzheimer's disease-like pathogenesis in vivo. We isolated (+)-taxifolin (4) from silymarin as an inhibitor of aggregation of the 42-residue amyloid β-protein. Structure-activity relationship studies revealed the 3',4'-dihydroxyl groups to be critical to the anti-aggregative ability, whereas the 7-hydroxyl group and the stereochemistry at positions 2 and 3 were not important.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Amyloid beta-Peptides / chemistry*
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Peptide Fragments / chemistry*
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Protein Multimerization / drug effects*
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Protein Structure, Secondary
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Quercetin / analogs & derivatives*
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Quercetin / chemistry
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Quercetin / isolation & purification
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Quercetin / pharmacology
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Silymarin / chemistry*
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Structure-Activity Relationship
Substances
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Amyloid beta-Peptides
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Peptide Fragments
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Silymarin
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amyloid beta-protein (1-42)
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Quercetin
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taxifolin