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学科主题: 药学
题名:
Neoechinulin B and its analogues as potential entry inhibitors of influenza viruses, targeting viral hemagglutinin
作者: Chen, Xueqing1; Si, Longlong1; Liu, Dong1; Proksch, Peter2; Zhang, Lihe1; Zhou, Demin1; Lin, Wenhan1
关键词: Prenylated indole diketopiperazines ; Neoechinulin B ; Eurotium rubrum ; Influenza virus entry inhibitor ; Hemagglutinin
刊名: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
发表日期: 2015-03-26
DOI: 10.1016/j.ejmech.2015.02.006
卷: 93, 页:182-195
收录类别: SCI ; IC
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Chemistry, Medicinal
研究领域[WOS]: Pharmacology & Pharmacy
关键词[WOS]: INDOLE DIKETOPIPERAZINE ALKALOIDS ; ASPERGILLUS-AMSTELODAMI ; FUNGUS ASPERGILLUS ; NEURAMINIDASE INHIBITOR ; ABSOLUTE-CONFIGURATION ; MEMBRANE-FUSION ; EUROTIUM SP ; CELL-DEATH ; ANTIINFLUENZA ; INFECTION
英文摘要:

A class of prenylated indole diketopiperazine alkaloids including 15 new compounds namely rubrum-lines A-O obtained from marine-derived fungus Eurotium rubrum, were tested against influenza A/WSN/33 virus. Neoechinulin B (18) exerted potent inhibition against H1N1 virus infected in MDCK cells, and is able to inhibit a panel of influenza virus strains including amantadine- and oseltamivir-resistant clinical isolates. Mechanism of action studies indicated that neoechinulin B binds to influenza envelope hemagglutinin, disrupting its interaction with the sialic acid receptor and the attachment of viruses to host cells. In addition, neoechinulin B was still efficient in inhibiting influenza A/WSN/33 virus propagation even after a fifth passage. The high potency and broad-spectrum activities against influenza viruses with less drug resistance make neoechinulin B as a new lead for the development of potential inhibitor of influenza viruses. (C) 2015 Elsevier Masson SAS. All rights reserved.

语种: 英语
所属项目编号: 2015CB755900 ; 2010CB12300 ; U1406402 ; 2011AA090701 ; 2013AA092902 ; DY125-15-T-01 ; GZ816 ; 81361168002 ; 81373271
项目资助者: National Basic Research Program 973 ; NSFC-Shangdong Join Fund for Marine Science ; National Hi-Tech 863-Projects ; COMRA ; Sino-German Project ; National Natural Science Foundation of China
WOS记录号: WOS:000351646100019
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/60819
Appears in Collections:北京大学药学院_期刊论文

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作者单位: 1.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
2.Univ Dusseldorf, Inst Pharmazeut Biol & Biotechnol, D-40225 Dusseldorf, Germany

Recommended Citation:
Chen, Xueqing,Si, Longlong,Liu, Dong,et al. Neoechinulin B and its analogues as potential entry inhibitors of influenza viruses, targeting viral hemagglutinin[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2015,93:182-195.
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