Publication: Anticholinesterase activity of 7-methoxyflavones isolated from Kaempferia parviflora
Issued Date
2009-12-01
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ISSN
10991573
0951418X
0951418X
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2-s2.0-73449085846
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Mahidol University
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SCOPUS
Bibliographic Citation
Phytotherapy Research. Vol.23, No.12 (2009), 1792-1794
Suggested Citation
Pattara Sawasdee, Chalisa Sabphon, Duangporn Sitthiwongwanit, Udom Kokpol Anticholinesterase activity of 7-methoxyflavones isolated from Kaempferia parviflora. Phytotherapy Research. Vol.23, No.12 (2009), 1792-1794. doi:10.1002/ptr.2858 Retrieved from: https://repository.li.mahidol.ac.th/handle/20.500.14594/28310
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Title
Anticholinesterase activity of 7-methoxyflavones isolated from Kaempferia parviflora
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Abstract
The rhizome of Kaempferia parviflora or kra-chai-dum (in Thai) is used traditionally as a folk medicine. The preliminary cholinesterase inhibitory screening of this plant extract exhibited significant acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities. Thirteen known methoxyflavones (1-13) were isolated and their structures were completely elucidated based on NMR analysis and compared with literature reports. Minor compounds 12-13 were reported for the first time from this species. The cholinesterase inhibitory test results showed that the highest potential inhibitors toward AChE and BChE were 5,7,4′-trimethoxyflavone (6) and 5,7-dimethoxyflavone (7), respectively, with the percentage inhibitory activity varying over 43-85%. The structure-activity relationship study led to the conclusion that compounds bearing 5,7-dimethoxy groups and a free substituent at C-3 had a significant inhibitory effect at a concentration of 0.1 mg/mL, but those bearing a 5-hydroxyl group reduced the inhibitory potency. On the other hand, flavones bearing a 3′- or 5′-methoxy group did not influence the inhibitory effect. Interestingly, 5,7-dimethoxyflavone (7) exhibited strong selectivity for BChE over AChE which may be of great interest to modify as a treatment agent for Alzheimer's disease. Copyright © 2009 John Wiley & Sons, Ltd.