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Title 

Cholinestrase inhibitory effects of geranylated flavonoids from Paulownia tomentosa fruits

 

오동나무 열매로부터 분리한 geranylated 플라보노이드의 cholinesterase 저해활성

Authors 

J K ChoYoung Bae RyuM J Curtis-LongH W RyuH J YukD W KimH J KimWoo Song LeeK H Park

Publisher 

Elsevier

Issue Date 

2012

Citation 

Bioorganic & Medicinal Chemistry, vol. 20, no. 8, pp. 2595-2602

Keywords 

ButyrylcholinesteraseFluorescence quenchingHuman acetylcholinesterasePaulownia tomentosaTime-dependent inhibitor --------------------------------------------------------------------------------

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.

ISSN 

0968-0896

Link 

http://dx.doi.org/10.1016/j.bmc.2012.02.044

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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