Synthesis of S-linked NeuAc-α(2-6)-di-LacNAc bearing liposomes for H1N1 influenza virus inhibition assays

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Bioorg Med Chem. 2018 Feb 12. pii: S0968-0896(17)32416-1. doi: 10.1016/j.bmc.2018.02.012. [Epub ahead of print]
[h=1]Synthesis of S-linked NeuAc-α(2-6)-di-LacNAc bearing liposomes for H1N1 influenza virus inhibition assays.[/h] Cheng HW[SUP]1[/SUP], Wang HW[SUP]1[/SUP], Wong TY[SUP]1[/SUP], Yeh HW[SUP]1[/SUP], Chen YC[SUP]1[/SUP], Liu DZ[SUP]2[/SUP], Liang PH[SUP]3[/SUP].
[h=3]Author information[/h]
[h=3]Abstract[/h] S-NeuAc-α(2-6)-di-LacNAc (5) was efficiently synthesized by a [2+2] followed by a [1+4] glycosylation, and later conjugated with 1,2-dilauroyl-sn-glycero-3-phosphoethanolamine (DLPE) to form both single-layer and multi-layer homogeneous liposomes in the presence of dipalmitoyl phosphatidylcholine (DPPC) and cholesterol. These liposomes were found to be weak inhibitors in both the influenza virus entry assay and the hemagglutination inhibition assay. The single layer liposome was found to more efficiently interfere with the entry of the H1N1 influenza virus into MDCK cells than the multilayer liposome containing 5.


[h=4]KEYWORDS:[/h] Hemagglutinin; Influenza; Liposome; Sialic acid

PMID: 29472127 DOI: 10.1016/j.bmc.2018.02.012