Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 18, Issue 23, Pages 6046-6049Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.10.033
Keywords
Neuraminidase; Pterocarpan; Sophora flavescens
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Funding
- KRIBB Research Instiative Program
- MOST/KOSEF to the Environmental Biotechnology National Core Research Center [R15-2003-012-020010]
- BK21 Program
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Pterocarpans (1-3) and flavanones (4-10) were isolated from Sophora flavescens and screened for their ability to inhibit neuraminidase (an enzyme crucial in the proliferation of the influenza virus). The majority of inhibitors were shown to have IC50 values of 20 mu M or below. Interestingly, pterocarpan 1 emerged as the best inhibitor with an IC50 of 1.4 mu M. We were thus able to prove that the pterocarpan skeleton is a new class of lead structure for neuraminidase inhibitors. Our studies reveal that the IC50 has a marked dependence upon structure in the case of the pterocarpans but much less so for the flavanones. Kinetic analysis disclosed that all inhibitors are noncompetitive. Our molecular docking experiment resulted that the most potent pterocarpan-derived inhibitor 1 may bind to another binding pocket adjacent to the active site. (C) 2008 Elsevier Ltd. All rights reserved.
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