Anticholinesterase activity of 7-methoxyflavones isolated from Kaempferia parviflora

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...

Full description

Saved in:

Bibliographic Details
Published in:	Phytotherapy research Vol. 23; no. 12; pp. 1792 - 1794
Main Authors:	Sawasdee, Pattara, Sabphon, Chalisa, Sitthiwongwanit, Duangporn, Kokpol, Udom
Format:	Journal Article
Language:	English
Published:	Chichester, UK John Wiley & Sons, Ltd 01-12-2009 Wiley
Subjects:	Acetylcholinesterase - metabolism anticholinesterase activity Apigenin - isolation & purification Apigenin - pharmacology Biological and medical sciences Butyrylcholinesterase - metabolism Cholinesterase Inhibitors - isolation & purification Cholinesterase Inhibitors - pharmacology Chromatography, High Pressure Liquid Flavonoids - isolation & purification Flavonoids - pharmacology General pharmacology Kaempferia parviflora Medical sciences Medicine, East Asian Traditional methoxyflavone Molecular Structure Pharmacognosy. Homeopathy. Health food Pharmacology. Drug treatments Plant Extracts - pharmacology Rhizome - chemistry Structure-Activity Relationship Zingiberaceae - chemistry Thailand Asia Monocotyledones Pharmacognosy Flavonoid Medicinal plant methoxyflavone Polyphenol Folk medicine Angiospermae Plant origin Phenols Flavone derivatives Spermatophyta Kaempferia parviflora anticholinesterase activity Anticholinesterase agent Zingiberaceae
Online Access:	Get full text
Tags:	Add Tag No Tags, Be the first to tag this record!

Description
Summary:	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.
Bibliography:	http://dx.doi.org/10.1002/ptr.2858 Thailand Research Fund (TRF) and the Commission on Higher Education (CHE) - No. MRG4980018 ark:/67375/WNG-NFRPDFRR-Q istex:4AFBE98AFE59CFD9D5FD5F30CFCC1DDFBE938C93 ArticleID:PTR2858 ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0951-418X 1099-1573
DOI:	10.1002/ptr.2858