Chalcones as novel influenza A (H1N1) neuraminidase inhibitors from Glycyrrhiza inflata
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- 作者：Trong Tuan Dao ; Phi Hung Nguyen ; Hong Sik Lee ; Eunhee Kim ; Junsoo Park ; Seong Il Lim ; Won Keun Oh
- 关键词：Glycyrrhiza inflata ; Licochalcone G ; Influenza A ; Novel influenza H1N1 ; Neuraminidase inhibitors ; Oseltamivir resistance
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2011
- 出版时间：1 January 2011
- 年：2011
- 卷：21
- 期：1
- 页码：294-298
- 全文大小：416 K
文摘
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 μM) 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.