Biological and Pharmaceutical Bulletin
Online ISSN : 1347-5215
Print ISSN : 0918-6158
ISSN-L : 0918-6158
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Monovalent Gb3-/Gb2-Derivatives Conjugated with a Phosphatidyl Residue: A Novel Class of Shiga Toxin-Neutralizing Agent
Paola NeriShunji TokoroShin-ichiro YokoyamaTsuyoshi MiuraTakeomi MurataYoshihiro NishidaTetsuya KajimotoSatoshi TsujinoToshiyuki InazuTaiichi UsuiHiroshi Mori
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2007 Volume 30 Issue 9 Pages 1697-1701

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Abstract

Shiga toxin (Stx) exerts toxic activity by binding to glycosphingolipids, mainly globotriaosyl (Gb3) ceramide, on the surface of target cells. The inhibition of toxin-receptor binding is a promising therapeutic approach to prevent Stx-mediated diseases. In this study, we synthesized monovalent Stx-ligands of phosphatidylethanolamine dipalmitoyl-Gb3 (Gb3-PEDP) and galabiosyl (Gb2)-PEDP and we examined their neutralizing activity against Stx-1 and Stx-2 in vitro. Both Gb3-PEDP and Gb2-PEDP strongly neutralized the cytotoxicity of Stx-1 and Stx-2. It is likely that the mechanism of neutralization involved formation of liposomes and consequently clustering of sugar units. We propose monovalent Gb3-/Gb2-derivatives conjugated with phosphatidyl residue as a novel class of Stx-neutralizing agent.

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© 2007 The Pharmaceutical Society of Japan
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