摘要：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.
