, Volume 15, Issue 5, pp 491-498

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

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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.