Glycoconjugate Journal

, Volume 15, Issue 5, pp 491–498 | Cite as

Development of glycosylated human interleukin-1α, neoglyco IL-1α, coupled with D-galactose monosaccharide: biological activities in vivo

  • Sachi Nabeshima
  • Taku Chiba
  • Yutaka Takei
  • Asako Ono
  • Kayoko Moriya
  • Kikuo Onozaki


In our previous study, a galactose monosaccharide with C9 spacer was chemically coupled to recombinant human interleukin 1α (rhIL-1α) in order to study the effect of glycosylation on its activities, and to develop IL-1 with less deleterious effects. The glycosylated IL-1α exhibited reduced activities in vitro by 10 to 10 000-fold depending upon different aspects of activities addressed. The affinity to type I and II IL-1 receptors were also reduced. In this study we examined a variety of IL-1 activities in vivo, including upregulation of serum levels of IL-6, α1-acid glycoprotein, NOx, corticosterone, downregulation of serum level of glucose, and recovery of peripheral white blood cells (WBCs) from myelosuppression in 5-fluorouracil-treated mice. In contrast to the biological activities in vitro, these activities in vivo were uniformly reduced by only about 10 to 20-fold compared to untreated IL-1α.

neoglycoprotein interleukin 1 cytokine 


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Copyright information

© Chapman and Hall 1998

Authors and Affiliations

  • Sachi Nabeshima
    • 1
  • Taku Chiba
    • 1
  • Yutaka Takei
    • 1
  • Asako Ono
    • 1
  • Kayoko Moriya
    • 1
  • Kikuo Onozaki
    • 1
  1. 1.Department of Hygienic Chemistry, Faculty of Pharmaceutical SciencesNagoya City UniversityTanabe, MizuhoNagoyaJapan

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