Structural characteristics of flavanones and flavones from Cudrania tricuspidata for neuraminidase inhibition

被引：44

作者：

Ryu, Young Bae ^{[1
]}

Curtis-Long, Marcus J.

Lee, Ji Won ^{[2
]}

Ryu, Hyung Won ^{[2
]}

Kim, Jun Young ^{[2
]}

Lee, Woo Song ^{[1
]}

Park, Ki Hun ^{[2
]}

机构：

[1] KRIBB, Bioind Technol & AI Control Biomat Res Ctr, Jeongeup 580185, South Korea

[2] Gyeongsang Natl Univ, Grad Sch, Inst Agr & Life Sci, Div Appl Life Sci,EB NCRC,Program BK21, Jinju 660701, South Korea

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 17期

关键词：

Neuraminidase; Cudrania tricuspidata; Flavonoid; TYROSINASE; XANTHONES; SIALIDASE;

D O I：

10.1016/j.bmcl.2009.07.098

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The structural characteristics of. avonoids (1-3 and 6-8) from the root of Cudrania tricuspidata required for neuraminidase inhibition were studied and compared with commercially available. avonoids (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. avanones (1-4) for neuraminidase in in silico docking experiments correlated well with their IC50 values and noncompetitive inhibition mode. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：4912 / 4915

页数：4

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