Untitled

Abstract

SLex-CMPul was found to have the potential to target drugs to the inflammatory lesion.

Sialyl Lewis X-Carboxymethylpullulan Conjugate: A Novel Homing Device to Spleen and Lymph Nodes

“…3) On the other hand, in these studies, we unexpectedly found that a significant amount of 2-3SLe x -CMPul was sequestered by the spleen but not CMPul, Neu5Ac-and SLN-CMPul. 5) Diethylaminoethyldextran 6) and dextran grafted onto poly-L-lysine 7) have already been reported to be preferentially taken up by the spleen and lymph nodes, but their amount in the spleen were much less than that of x -CMPul.…”

“…x moiety in 2-3SLe x -CMPul was recognized by E-selectin 3) and the fucose and 2-3 linked sialic acid that are essential sugar residues for binding to selectins were structurally required for the accumulation in the peripheral lymphoid tissues. 2) However, E-and P-selectins are not thought to be constitutively expressed in normal spleen and lymph nodes.…”

“…These oligosaccharide-CMPul conjugates were labeled with 3 H for the tissue distribution experiments as described previously.…”

“…Microautoradiography Female Lewis rats (150-170 g body weight: age 7 weeks) were used for microautoradiography analyses at the cellular level. After anesthesia with diethyl ether, 3 H-labeled CMPul or oligosaccharide-CMPul conjugates, with specific activities of approximately 3 mCi/0.5 mg/ml were administered intravenously at a dose of 2 ml/kg to rats. The rats were anesthetized again and exsanguinated through the veva cava at 2 h or 24 h after intravenous administration.…”

“…3) This conjugate had E-selectin binding activity and a prolonged circulating time due to the presence of the 2-3SLe…”