lewis-x-antigen and Pleurisy

Sialyl Lewis X (1) is known to be a ligand of the cell adhesion molecule E-selectin. We have synthesized several biantennary glycoside-terminated ligands mimicking sialyl Lewis X (1), and evaluated their binding activity to E-selectin using HL-60 cells expressing sialyl Lewis X epitope and human umbilical vein endothelial cells (HUVECs). These compounds were found to possess moderate binding activities to E-selectin. Among them, di-fucoside analog (8) which has no sialic acid carboxylate group was more active than 2, which had both the sialyl-galactose residue and the fucose residue (IC50, 8: 4.7 mM, 2: 11.7 mM). Furthermore, in the rat pleuritic model in vivo induced by carrageenin, 8 was found to reduce neutrophil infiltration at inflammatory lesions.

Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Carbohydrate Sequence; Carrageenan; Cell Adhesion; Cell Line; Chemical Phenomena; Chemistry, Physical; Humans; Lewis X Antigen; Ligands; Molecular Conformation; Molecular Sequence Data; Oligosaccharides; Pleurisy; Rats; Receptors, Cell Surface; Sialyl Lewis X Antigen