Synthesis of sialyl Lewis X-polysaccharide conjugates

Article abstract of DOI:10.1248/cpb.48.1256

Sialyl Lewis X (SLe(x)) is well known as a ligand of the cell adhesion molecule E-selectin which is specifically expressed at inflammatory lesion sites. We have synthesized several SLe(x)-polysaccharide conjugates and examined their potential for drug delivery to inflammatory lesions. The AUC (area under the blood concentration-time curve) 0 - 24 h of SLe(x)-CMCht (1), SLe(x)-CMPul (2) and SLe(x)-DSH (3) at the inflammatory lesion was about 60-, 300-, and 30-fold higher than that of the monovalent SLe(x) (7), respectively. Moreover, 1 showed 2-fold higher accumulation in the inflammatory lesion than SLN-CMCht (4), and 2 showed 2.5-fold higher accumulation than SLN-CMPul (5).