Cholinestrase inhibitory effects of geranylated flavonoids from Paulownia tomentosa fruits = 오동나무 열매로부터 분리한 geranylated 플라보노이드의 cholinesterase 저해활성

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Title
Cholinestrase inhibitory effects of geranylated flavonoids from Paulownia tomentosa fruits = 오동나무 열매로부터 분리한 geranylated 플라보노이드의 cholinesterase 저해활성
Author(s)
J K Cho; Young Bae Ryu; M J Curtis-Long; Hyung Won Ryu; H J Yuk; D W Kim; H J Kim; Woo Song Lee; K H Park
Bibliographic Citation
Bioorganic & Medicinal Chemistry, vol. 20, no. 8, pp. 2595-2602
Publication Year
2012
Abstract
Alzheimer's disease is rapidly becoming one of the most prevalent human diseases. Inhibition of human acetylcholinestrase (hAChE) and butyrylcholinestrase (BChE) has been linked to amelioration of Alzheimer's symptoms and research into inhibitors is of critical importance. Purification of the methanol extract of Paulownia tomentosa fruits yielded potent hAChE and BChE inhibitoryflavonoids (1-9). A comparative activity screen indicated that a geranyl group at C6 is crucial for both hAChE and BChE. For example, diplacone (8) showed 250-fold higher efficacy than its parent eriodictyol (12). IC 50s of diplacone (8) were 7.2 μM for hAChE and 1.4 μM for BChE. Similar trends were also observed for 4′-O-methyldiplacone (4) (vs its parent, hesperetin 10) and mimulone (7) (vs its parent, naringenin 11). Representative inhibitors (1-8) showed mixed inhibition kinetics as well as time-dependent, reversible inhibition toward hAChE. The binding affinities of these compounds to hAChE were investigated by monitoring quenching of inherent enzyme fluorescence. The affinity constants (K SA) increased in proportion to inhibitory potencies.
Keyword
ButyrylcholinesteraseFluorescence quenchingHuman acetylcholinesterasePaulownia tomentosaTime-dependent inhibitor
ISSN
0968-0896
Publisher
Elsevier
DOI
http://dx.doi.org/10.1016/j.bmc.2012.02.044
Type
Article
Appears in Collections:
Jeonbuk Branch Institute > Functional Biomaterial Research Center > 1. Journal Articles
Ochang Branch Institute > Natural Product Research Center > 1. Journal Articles
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