tetano
Editor, Senior Moderator
Eur J Med Chem. 2015 Feb 7;93C:182-195. doi: 10.1016/j.ejmech.2015.02.006. [Epub ahead of print]
[h=1]Neoechinulin B and its analogues as potential entry inhibitors of influenza viruses, targeting viral hemagglutinin.[/h] Chen X[SUP]1[/SUP], Si L[SUP]1[/SUP], Liu D[SUP]1[/SUP], Proksch P[SUP]2[/SUP], Zhang L[SUP]1[/SUP], Zhou D[SUP]3[/SUP], Lin W[SUP]4[/SUP].
[h=3]Author information[/h]
[h=3]Abstract[/h] A class of prenylated indole diketopiperazine alkaloids including 15 new compounds namely rubrumlines 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.
Copyright ? 2015 Elsevier Masson SAS. All rights reserved.
[h=4]KEYWORDS:[/h] Eurotium rubrum; Hemagglutinin; Influenza virus entry inhibitor; Neoechinulin B; Prenylated indole diketopiperazines
PMID: 25681711 [PubMed - as supplied by publisher]
[h=1]Neoechinulin B and its analogues as potential entry inhibitors of influenza viruses, targeting viral hemagglutinin.[/h] Chen X[SUP]1[/SUP], Si L[SUP]1[/SUP], Liu D[SUP]1[/SUP], Proksch P[SUP]2[/SUP], Zhang L[SUP]1[/SUP], Zhou D[SUP]3[/SUP], Lin W[SUP]4[/SUP].
[h=3]Author information[/h]
[h=3]Abstract[/h] A class of prenylated indole diketopiperazine alkaloids including 15 new compounds namely rubrumlines 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.
Copyright ? 2015 Elsevier Masson SAS. All rights reserved.
[h=4]KEYWORDS:[/h] Eurotium rubrum; Hemagglutinin; Influenza virus entry inhibitor; Neoechinulin B; Prenylated indole diketopiperazines
PMID: 25681711 [PubMed - as supplied by publisher]