Abstract
The synthesis of a water/plasma soluble, noncytotoxic, "clicked" sugar-derivative of curcumin with amplified bioefficacy in modulating amyloid-β and tau peptide aggregation is presented. Curcumin inhibits amyloid-β and tau peptide aggregation at micromolar concentrations; the sugar-curcumin conjugate inhibits Aβ and tau peptide aggregation at concentrations as low as 8 nM and 0.1 nM, respectively. In comparison to curcumin, this conveniently synthesized Alzheimer's drug candidate is a more powerful antioxidant.
Keywords:
Alzheimer’s disease (AD); amyloid-β; antioxidant potential; curcumin; tau peptide; “click” reaction.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Alzheimer Disease / drug therapy
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Alzheimer Disease / metabolism
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Amyloid beta-Peptides / metabolism*
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Animals
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Antioxidants / administration & dosage
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Antioxidants / chemical synthesis
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Antioxidants / metabolism
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Cells, Cultured
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Curcumin / administration & dosage
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Curcumin / chemical synthesis*
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Curcumin / metabolism*
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Galactose / administration & dosage
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Galactose / chemical synthesis*
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Galactose / metabolism*
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Hippocampus / drug effects
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Hippocampus / metabolism
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Humans
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Mice
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tau Proteins / metabolism*
Substances
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Amyloid beta-Peptides
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Antioxidants
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tau Proteins
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Curcumin
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Galactose