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Structural characteristics of flavanones and flavones from Cudrania tricuspidata for neuraminidase inhibition
- Authors
- Ryu, Young Bae; Curtis-Long, Marcus J.; Lee, Ji Won; Ryu, Hyung Won; Kim, Jun Young; Lee, Woo Song; Park, Ki Hun
- Issue Date
- 1-Sep-2009
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- Neuraminidase; Cudrania tricuspidata; Flavonoid
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.19, no.17, pp 4912 - 4915
- Pages
- 4
- Indexed
- SCIE
SCOPUS
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Volume
- 19
- Number
- 17
- Start Page
- 4912
- End Page
- 4915
- ISSN
- 0960-894X
1464-3405
- Abstract
- 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.
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