Anticholinesterase activity of plastoquinones from  Sargassum sagamianum : lead compounds for alzheimer's disease therapy | Zendy

Choi Byoung Wook | Zendy; Ryu Geonseek | Zendy; Park Soo Hee | Zendy; Kim Eun Sook | Zendy; Shin Jongheon | Zendy; Roh Seok Seon | Zendy; Shin Hyeon Cheol | Zendy; Lee Bong Ho | Zendy

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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.

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