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Chemoenzymatic synthesis and application of glycopolymers containing multivalent sialyloligosaccharides with a poly(L-glutamic acid) backbone for inhibition of infection by influenza viruses

Glycobiology. 2003 May;13(5):315-26. doi: 10.1093/glycob/cwg032. Epub 2002 Dec 17.

Abstract

Highly water-soluble glycopolymers with poly(alpha-L-glutamic acid) (PGA) backbones carrying multivalent sialyl oligosaccharides units were chemoenzymatically synthesized as polymeric inhibitors of infection by human influenza viruses. p-Aminophenyl disaccharide glycosides were coupled with gamma-carboxyl groups of PGA side chains and enzymatically converted to Neu5Acalpha2-3Galbeta1-4GlcNAcbeta-, Neu5Acalpha2-6Galbeta1-4GlcNAcbeta-, Neu5Acalpha2-3Galbeta1-3GalNAcalpha-, and Neu5Acalpha2-3Galbeta1-3GalNAcbeta- units, respectively, by alpha2,3- or alpha2,6-sialytransferases. The glycopolymers synthesized were used for neutralization of human influenza A and B virus infection as assessed by measurement of the degree of cytopathic inhibitory effect in virus-infected MDCK cells. Among the glycopolymers tested, alpha2,6-sialo-PGA with a high molecular weight (260 kDa) most significantly inhibited infection by an influenza A virus, strain A/Memphis/1/71 (H3N2), which predominantly binds to alpha2-6 Neu5Ac residue. The alpha2,6-sialo-PGA also inhibited infection by an influenza B virus, B/Lee/40. The binding preference of viruses to terminal sialic acids was affected by core determinants of the sugar chain, Galbeta1-4GlcNAcbeta- or Galbeta1-3GalNAcalpha/beta- units. Inhibition of infection by viruses was remarkably enhanced by increasing the molecular weight and sialic acid content of glycopolymers.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Carbohydrate Sequence
  • Cells, Cultured
  • Cytotoxicity Tests, Immunologic
  • Dogs
  • Immune Sera / pharmacology
  • Influenza A virus* / drug effects
  • Influenza A virus* / physiology
  • Influenza B virus* / drug effects
  • Influenza B virus* / physiology
  • Mice
  • Molecular Sequence Data
  • Oligosaccharides / chemical synthesis*
  • Oligosaccharides / immunology
  • Oligosaccharides / pharmacology
  • Orthomyxoviridae Infections / prevention & control*
  • Polyglutamic Acid / chemistry*
  • Polysaccharides / chemical synthesis*
  • Polysaccharides / immunology
  • Polysaccharides / pharmacology
  • Sialoglycoproteins / chemical synthesis*
  • Sialoglycoproteins / immunology
  • Structure-Activity Relationship

Substances

  • Immune Sera
  • Oligosaccharides
  • Polysaccharides
  • Sialoglycoproteins
  • sialooligosaccharides
  • Polyglutamic Acid