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Abstract Title:

Pterocarpans and flavanones from Sophora flavescens displaying potent neuraminidase inhibition.

Abstract Source:

Bioorg Med Chem Lett. 2008 Dec 1;18(23):6046-9. Epub 2008 Oct 11. PMID: 18938076

Abstract Author(s):

Young Bae Ryu, Marcus J Curtis-Long, Jin Hyo Kim, Seong Hun Jeong, Min Suk Yang, Keun Woo Lee, Woo Song Lee, Ki Hun Park

Abstract:

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 IC(50) values of 20 microM or below. Interestingly, pterocarpan 1 emerged as the best inhibitor with an IC(50) of 1.4 microM. 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 IC(50) 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.

Study Type : In Vitro Study

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Sayer Ji
Founder of GreenMedInfo.com

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