Abstract
P-selectin blocking potency was investigated using synthetic monomeric and polymeric anionic compounds containing sulfate groups such as O-sulfotyrosine (sTyr) and/or sulfated Lewis structures. A non-carbohydrate-containing polyacrylamide conjugate sTyr–PAA (80% mol of sTyr) was a remarkably potent inhibitor of P-selectin binding in vitro, having an IC 50 value of 6 ng/mL (equivalent to 10 nM calculated on the basis of sTyr residues or 0.1 nM calculated by the mass of the macromolecule). The inhibitory effect of sTyr–PAA (80%) towards P-selectin is significantly greater than that of fucoidan (IC 50, 100 ng/mL). However, sTyr–PAA (80%) was less effective than fucoidan at reducing neutrophil extravasation in an in vivo rat model of peritonitis.
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