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Anticholinesterase activity of plastoquinones from Sargassum sagamianum : lead compounds for alzheimer's disease therapy
Author(s) -
Choi Byoung Wook,
Ryu Geonseek,
Park Soo Hee,
Kim Eun Sook,
Shin Jongheon,
Roh Seok Seon,
Shin Hyeon Cheol,
Lee Bong Ho
Publication year - 2007
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.2090
Subject(s) - butyrylcholinesterase , acetylcholinesterase , aché , potency , sargassum , pharmacology , inhibitory postsynaptic potential , drug , cholinesterase , chemistry , medicine , biology , enzyme , biochemistry , in vitro , botany , algae
During the search for anticholinesterase compounds from marine organisms, two known plastoquinones, sargaquinoic acid (1) and sargachromenol (2), were isolated from Sargassum sagamianum . Both compounds showed moderate acetylcholinesterase (AChE) inhibitory activity in a micromole range (IC 50 23.2 and 32.7 µ m , respectively). However, for butyrylcholinesterase (BuChE), a new target for the treatment of Alzheimer's disease (AD), compound 1 showed particularly potent inhibitory activity (IC 50 26 n m ), which is 1000‐fold greater than for AChE. Hence, sargaquinoic acid represents an effective and selective inhibitor of BuChE with a potency similar to or greater than the anticholinesterases in current clinical use, making it an interesting potential drug candidate for AD. Copyright © 2007 John Wiley & Sons, Ltd.