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

TY - JOUR

T1 - Chalcones as novel influenza A (H1N1) neuraminidase inhibitors from Glycyrrhiza inflata

AU - Dao, Trong Tuan

AU - Nguyen, Phi Hung

AU - Lee, Hong Sik

AU - Kim, Eunhee

AU - Park, Junsoo

AU - Lim, Seong Il

AU - Oh, Won Keun

N1 - Copyright © 2010 Elsevier Ltd. All rights reserved.

PY - 2011/1/1

Y1 - 2011/1/1

N2 - 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.

AB - 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.

KW - Amino Acid Substitution

KW - Antiviral Agents

KW - Cell Line

KW - Chalcones

KW - Drug Resistance, Viral

KW - Enzyme Inhibitors

KW - Glycyrrhiza

KW - Humans

KW - Influenza A Virus, H1N1 Subtype

KW - Influenza A Virus, H9N2 Subtype

KW - Magnetic Resonance Spectroscopy

KW - Molecular Conformation

KW - Mutation

KW - Neuraminidase

KW - Journal Article

KW - Research Support, Non-U.S. Gov't

U2 - 10.1016/j.bmcl.2010.11.016

DO - 10.1016/j.bmcl.2010.11.016

M3 - Journal article

C2 - 21123068

SN - 0960-894X

VL - 21

SP - 294

EP - 298

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

IS - 1

ER -