title: Anticholinesterase activity of plastoquinones from Sargassum sagamianum: lead compounds for Alzheimer's disease therapy.
abstract: 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 microm, 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 nm), 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.
authors.affiliation: Laboratory of Aging and Degenerative Disease and Department of Applied Chemistry, Hanbat National University, 16-1 Dukmyung-dong, Yuseong-gu, Daejeon, Korea.
authors.forename: Byoung Wook
authors.initials: BW
authors.lastname: Choi
authors.forename: Geonseek
authors.initials: G
authors.lastname: Ryu
authors.forename: Soo Hee
authors.initials: SH
authors.lastname: Park
authors.forename: Eun Sook
authors.initials: ES
authors.lastname: Kim
authors.forename: Jongheon
authors.initials: J
authors.lastname: Shin
authors.forename: Seok Seon
authors.initials: SS
authors.lastname: Roh
authors.forename: Hyeon Cheol
authors.initials: HC
authors.lastname: Shin
authors.forename: Bong Ho
authors.initials: BH
authors.lastname: Lee
mesh_terms: D000110:Acetylcholinesterase / Q000737:chemistry; D000475:Alkenes / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D000544:Alzheimer Disease / Q000188:drug therapy*; D001578:Benzopyrans / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D016227:Benzoquinones / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D002091:Butyrylcholinesterase / Q000737:chemistry; D002800:Cholinesterase Inhibitors / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D008517:Phytotherapy; D044647:Sargassum / Q000737:chemistry*
chemical_list: D000475:Alkenes; D001578:Benzopyrans; D016227:Benzoquinones; D002800:Cholinesterase Inhibitors; C503204:sargachromenol; C477718:sargaquinoic acid; D000110:Acetylcholinesterase; D002091:Butyrylcholinesterase