4.5 Article

Chalcones as novel influenza A (H1N1) neuraminidase inhibitors from Glycyrrhiza inflata

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 21, Issue 1, Pages 294-298

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.11.016

Keywords

Glycyrrhiza inflata; Licochalcone G; Influenza A; Novel influenza H1N1; Neuraminidase inhibitors; Oseltamivir resistance

Funding

  1. Korean government (MOST) [M10642140004-06N4214-00410]
  2. Korea Science and Engineering Foundation (KOSEF), Ministry for Food, Agriculture, Forestry and Fisheries, Republic of Korea

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The emergence of highly pathogenic influenza A virus strains, such as the new H1N1 swine influenza (novel influenza), represents a serious threat to global human health. During our course of an anti-influenza screening program on natural products, one new licochalcone G(1) and seven known (2-8) chalcones were isolated as active principles from the acetone extract of Glycyrrhiza inflata. Compounds 3 and 6 without prenyl group showed strong inhibitory effects on various neuraminidases from influenza viral strains, H1N1, H9N2, novel H1N1 (WT), and oseltamivir-resistant novel H1N1 (H274Y) expressed in 293T cells. In addition, the efficacy of oseltamivir with the presence of compound 3 (5 mu M) was increased against H274Y neuraminidase. This evidence of synergistic effect makes this inhibitor to have a potential possibility for control of pandemic infection by oseltamivir-resistant influenza virus. (C) 2010 Elsevier Ltd. All rights reserved.

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