Abstract
A series of 9-N-substituted berberine derivatives were synthesized and biologically evaluated as antioxidant and inhibitors of acetylcholinesterase (AChE), butyrylcholinesterase and amyloid-β aggregation. Most of these compounds exhibited very good antioxidant activities, inhibitive activities of AChE and amyloid-β aggregation. Among them, compound 8d, (o-methylphenethyl)amino linked at the 9-position of berberine, was found to be a good antioxidant (with 4.05 μM of Trolox equivalents), potent inhibitor of AChE (an IC(50) value of 0.027 μM), and high active inhibitor of amyloid-β aggregation (an IC(50) value of 2.73 μM).
Copyright © 2011 Elsevier Masson SAS. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Acetylcholinesterase / metabolism
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Alzheimer Disease / drug therapy
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Alzheimer Disease / metabolism
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Amyloid beta-Peptides / antagonists & inhibitors*
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Amyloid beta-Peptides / metabolism
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Animals
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Antioxidants / chemical synthesis
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Antioxidants / chemistry*
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Antioxidants / pharmacology*
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Berberine / analogs & derivatives*
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Berberine / chemical synthesis
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Berberine / pharmacology*
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Butyrylcholinesterase / metabolism
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Cholinesterase Inhibitors / chemical synthesis
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Cholinesterase Inhibitors / chemistry*
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Cholinesterase Inhibitors / pharmacology*
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Electrophorus
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Horses
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Humans
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Models, Molecular
Substances
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Amyloid beta-Peptides
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Antioxidants
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Cholinesterase Inhibitors
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Berberine
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Acetylcholinesterase
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Butyrylcholinesterase