Prolyl endopeptidase inhibitory activity of chitosan sulfates with different degree of deacetylation

Three kinds of partially deacetylated chitosan, 90% deacetylated chitosan, 75% deacetylated chitosan and 50% deacetylated chitosan, were prepared from crab chitin by N-deacetylation with 40% (w/w) sodium hydroxide solution for different durations. In order to improve biological activity and solubility, their sulfated derivatives were prepared, and prolyl endopeptidase (PEP) inhibitory activities were investigated. Fifty percent-deacetylated chitosan sulfate (50-CS) exhibited the highest inhibitory activity, and inhibition rate was a dose-dependant. In addition, Dixon plots suggested that 50-CS was act as competitive inhibitor, and the inhibition constant (K-i) was 2.6 mg/ml. (c) 2005 Elsevier Ltd. All rights reserved.