Multifunctional Activity of Polyphenolic Compounds Associated with a Potential for Alzheimer's Disease Therapy from Ecklonia cava
Copyright policy )Multifunctional Activity of Polyphenolic Compounds Associated with a Potential for Alzheimer's Disease Therapy from Ecklonia cava
Five polyphenols were isolated and purified from a brown alga Ecklonia cava. These compounds showed diverse biological activities such as antioxidative, antiinflammatory, and enzyme inhibitory activities. This led us to investigate the potential of these compounds as Alzheimer's disease drugs. All of the compounds showed moderate acetylcholinesterase inhibitory activity in a micromolar range (IC50 from 16.0 to 96.3 μM). For butyrylcholinesterase, a new target for the treatment of Alzheimer's disease, phlorofucofuroeckol‐A (PFF‐A), showed a particularly potent inhibitory activity (IC50 0.95 μM), which is over 100‐fold greater than for acetylcholinesterase. These compounds inhibited glycogen synthase kinase 3 beta, which is related to the formation of hyperphosphorylated tau and generation Aβ. Bieckol and PFF‐A inhibited amyloid precursor protein biosynthesis. PFF‐A also showed very strong β‐secretase inhibitory activity with IC50 of submicromole. These results render these compounds as interesting potential drug candidates for Alzheimer's disease. Copyright © 2015 John Wiley & Sons, Ltd.
- SUNY Korea Korea (Republic of)
- State University of New York at Potsdam United States
- State University of New York United States
- Hanbat National University Korea (Republic of)
Amyloid beta-Peptides, Glycogen Synthase Kinase 3 beta, Phaeophyceae, Polyphenols, Dioxins, Cell Line, Glycogen Synthase Kinase 3, Alzheimer Disease, Butyrylcholinesterase, Acetylcholinesterase, Humans, Cholinesterase Inhibitors, Amyloid Precursor Protein Secretases, Benzofurans
Amyloid beta-Peptides, Glycogen Synthase Kinase 3 beta, Phaeophyceae, Polyphenols, Dioxins, Cell Line, Glycogen Synthase Kinase 3, Alzheimer Disease, Butyrylcholinesterase, Acetylcholinesterase, Humans, Cholinesterase Inhibitors, Amyloid Precursor Protein Secretases, Benzofurans
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