title: Multifunctional activity of polyphenolic compounds associated with a potential for Alzheimer's disease therapy from Ecklonia cava.
abstract: 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.
authors: Department of Chemical and Biological Engineering, Hanbat National University, Dongseodaero 125, Yuseong-gu, Daejeon,, 305-719, Korea.
authors: Byoung Wook
authors: BW
authors: Choi
authors: Hye Sook
authors: HS
authors: Lee
authors: Hyeon-Cheol
authors: HC
authors: Shin
authors: Bong Ho
authors: BH
authors: Lee
mesh_terms: D000110:Acetylcholinesterase / Q000378:metabolism; D000544:Alzheimer Disease / Q000188:drug therapy; D053829:Amyloid Precursor Protein Secretases / Q000037:antagonists & inhibitors*; D016229:Amyloid beta-Peptides / Q000096:biosynthesis; D001572:Benzofurans / Q000494:pharmacology*; D002091:Butyrylcholinesterase / Q000378:metabolism; D002460:Cell Line; D002800:Cholinesterase Inhibitors / Q000494:pharmacology*; D004147:Dioxins / Q000494:pharmacology*; D038362:Glycogen Synthase Kinase 3 / Q000037:antagonists & inhibitors; D000071679:Glycogen Synthase Kinase 3 beta; D006801:Humans; D000459:Phaeophyceae / Q000737:chemistry*; D059808:Polyphenols / Q000494:pharmacology*
chemical_list: D016229:Amyloid beta-Peptides; D001572:Benzofurans; D002800:Cholinesterase Inhibitors; D004147:Dioxins; D059808:Polyphenols; C064093:phlorofucofuroeckol A; C000605506:GSK3B protein, human; D000071679:Glycogen Synthase Kinase 3 beta; D038362:Glycogen Synthase Kinase 3; D000110:Acetylcholinesterase; D002091:Butyrylcholinesterase; D053829:Amyloid Precursor Protein Secretases
keywords: APP; Ecklonia cava; GSK3β; cholinesterases; polyphenols; β-secretase