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In vitro biological activities of glycosylated human interleukin-1α, neoglyco IL-1α, coupled with N-acetylneuraminic acid

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Abstract

In the previous study, N-acetylneuraminic acid (NANA) with C9 spacer was chemically coupled to human recombinant (rh) IL-1α in order to study the effect of glycosylation on its biological activities, and to develop IL-1 with less deleterious effects. In this study we examined a variety of IL-1 activities in vitro, including proliferative effect on T cells, antiproliferative effect on myeloid leukemic cells and melanoma cells, stimulatory effects on IL-6 synthesis by melanoma cells and PGE2 synthesis by fibroblast cells. NANA-introduced IL-1α (NANA-IL-1α) exhibited reduced activities about ten times compared with original IL-1α in all the activities performed in vitro. The competitive binding of 125I-IL-1α to mouse T cells and pre-B cells with unlabeled IL-1αs suggests the decrease in binding affinities of NANA-IL-1α to both type I and type II IL-1 receptors. Therefore, reduced activities of NANA-IL-1α well correlated with the decrease in its receptor binding affinities.

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Authors and Affiliations

  1. Department of Hygeinic Chemistry, Faculty of Pharmaceutical Sciences, Nagoya City University, Tanabe, Mizuho, Nagoya, 467-8603, Japan

    Kayoko Moriya, Taku Chiba, Sachi Nabeshima, Hidetoshi Hayashi & Kikuo Onozaki

Authors
  1. Kayoko Moriya
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  2. Taku Chiba
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  3. Sachi Nabeshima
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  4. Hidetoshi Hayashi
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  5. Kikuo Onozaki
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Moriya, K., Chiba, T., Nabeshima, S. et al. In vitro biological activities of glycosylated human interleukin-1α, neoglyco IL-1α, coupled with N-acetylneuraminic acid. Glycoconj J 16, 563–568 (1999). https://doi.org/10.1023/A:1007082207188

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