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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 32, Number 8
BKCSDE 32(8)
August 20, 2011 

Development of selective butyrylcholinesterase inhibitors using (R)-lipoic acid-polyphenol hybrid molecules
Yeun Ji Woo, Bo Hyun Lee, Go Heum Yeun, Hyun Ju Kim, Jang Myoun Ko, Moo-Ho Won, Bong Ho Lee, Jeong Ho Park *
Molecular hybridization, (R)-Lipoic acid, Polyphenols, Cholinesterase inhibitor
A series of hybrid molecules between (R)-lipoic acid (ALA) and the acetylated or methylated polyphenol compounds were synthesized and their in vitro cholinesterase [acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE)] inhibition activities were checked. The IC50 values of all hybrid molecules for a BuChE inhibition were lower than those of the single parent compounds. Specifically, ALA-acetyl protected caffeic acid (11, ALA-AcCA) was shown as an effective inhibitor of BuChE (IC50 = 0.5 ± 0.2 μM) and also had a great selectivity for BuChE over AChE (more than 800 fold). Inhibition kinetic study indicated that 11 is a mixed inhibition type. Its binding affinity (Ki) value to BuChE is 1.52 ± 0.18 μM.
2997 - 3002
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