Structural characteristics of flavanones and flavones from Cudrania tricuspidata for neuraminidase inhibition = 꾸지뽕나무 뿌리로 부터 뉴라미니데이즈 제해제 개발

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Title
Structural characteristics of flavanones and flavones from Cudrania tricuspidata for neuraminidase inhibition = 꾸지뽕나무 뿌리로 부터 뉴라미니데이즈 제해제 개발
Author(s)
Young Bae Ryu; M J Curtis-Long; J W Lee; Hyung Won Ryu; J Y Kim; Woo Song Lee; K H Park
Bibliographic Citation
Bioorganic & Medicinal Chemistry Letters, vol. 19, no. 17, pp. 4912-4915
Publication Year
2009
Abstract
The structural characteristics of flavonoids (1.3 and 6.8) from the root of Cudrania tricuspidata required for neuraminidase inhibition were studied and compared with commercially available flavonoids (4, 5, and 9.12). Alkylated flavanones (1.3) display better inhibition than the corresponding parent compound 4. Importantly, flavanone 1 bearing a C-8 hydrated prenyl group showed extremely high inhibition with IC50 of 380 nM. On the other hand, the parent flavone 5 was more effective than alkylated analogues (6.8). Isolated inhibitors (1.3 and 6.8) showed noncompetitive inhibition in kinetic studies. The binding affinity of flavanones (1.4) for neuraminidase in in silico docking experiments correlated well with their IC50 values and noncompetitive inhibition mode.
Keyword
NeuraminidaseCudrania tricuspidataFlavonoid
ISSN
0960-894X
Publisher
Elsevier
DOI
http://dx.doi.org/10.1016/j.bmcl.2009.07.098
Type
Article
Appears in Collections:
Jeonbuk Branch Institute > Functional Biomaterial Research Center > 1. Journal Articles
Ochang Branch Institute > Natural Medicine Research Center > 1. Journal Articles
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