Development of selective butyrylcholinesterase inhibitors using (R)-lipoic acid-polyphenol hybrid molecules 


Vol. 32,  No. 8, pp. 2997-3002, Aug.  2011
10.5012/bkcs.2011.32.8.2997


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  Abstract

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.

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  Cite this article

[IEEE Style]

Y. J. Woo, B. H. Lee, G. H. Yeun, H. J. Kim, J. M. Ko, M. Won, B. H. Lee, J. H. Park, "Development of selective butyrylcholinesterase inhibitors using (R)-lipoic acid-polyphenol hybrid molecules," Bulletin of the Korean Chemical Society, vol. 32, no. 8, pp. 2997-3002, 2011. DOI: 10.5012/bkcs.2011.32.8.2997.

[ACM Style]

Yeun Ji Woo, Bo Hyun Lee, Go Heum Yeun, Hyun Ju Kim, Jang Myoun Ko, Moo-Ho Won, Bong Ho Lee, and Jeong Ho Park. 2011. Development of selective butyrylcholinesterase inhibitors using (R)-lipoic acid-polyphenol hybrid molecules. Bulletin of the Korean Chemical Society, 32, 8, (2011), 2997-3002. DOI: 10.5012/bkcs.2011.32.8.2997.

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ISSN(Print) 0253-2964
ISSN(Online) 1229-5949