Format

Send to

Choose Destination
Biol Pharm Bull. 2007 Sep;30(9):1697-701.

Monovalent Gb3-/Gb2-derivatives conjugated with a phosphatidyl residue: a novel class of Shiga toxin-neutralizing agent.

Author information

1
Laboratory of Microbiology, Department of Public Health Pharmacy, Gifu Pharmaceutical University, Gifu 502-8585, Japan.

Abstract

Shiga toxin (Stx) exerts toxic activity by binding to glycosphingolipids, mainly globotriaosyl (Gb(3)) 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-Gb(3) (Gb(3)-PEDP) and galabiosyl (Gb(2))-PEDP and we examined their neutralizing activity against Stx-1 and Stx-2 in vitro. Both Gb(3)-PEDP and Gb(2)-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 Gb(3)-/Gb(2)-derivatives conjugated with phosphatidyl residue as a novel class of Stx-neutralizing agent.

PMID:
17827723
DOI:
10.1248/bpb.30.1697
[Indexed for MEDLINE]
Free full text

Supplemental Content

Full text links

Icon for J-STAGE, Japan Science and Technology Information Aggregator, Electronic
Loading ...
Support Center