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Multifunctional Activity of Polyphenolic Compounds Associated with a Potential for Alzheimer's Disease Therapy from Ecklonia cava
Author(s) -
Choi Byoung Wook,
Lee Hye Sook,
Shin HyeonCheol,
Lee Bong Ho
Publication year - 2015
Publication title -
phytotherapy research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.019
H-Index - 129
eISSN - 1099-1573
pISSN - 0951-418X
DOI - 10.1002/ptr.5282
Subject(s) - acetylcholinesterase , butyrylcholinesterase , pharmacology , polyphenol , biochemistry , enzyme , aché , chemistry , gsk 3 , alzheimer's disease , amyloid precursor protein , biology , medicine , kinase , disease , antioxidant
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 (IC 50 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 (IC 50 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 IC 50 of submicromole. These results render these compounds as interesting potential drug candidates for Alzheimer's disease. Copyright © 2015 John Wiley & Sons, Ltd.