Synthesis of sialyl Lewis X-polysaccharide conjugates |
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Authors: | Sakagami M Horie K Nakamoto K Kawaguchi T Hamana H |
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Affiliation: | Drug Delivery System Institute, Ltd., Noda, Chiba, Japan. masahiro.sakagami@shionogi.co.jp |
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Abstract: | Sialyl Lewis X (SLeX) 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 SLeX-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 SLeX-CMCht (1), SLeX-CMPul (2) and SLeX-DSH (3) at the inflammatory lesion was about 60-, 300-, and 30-fold higher than that of the monovalent SLeX (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). |
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