Influence of the oversulfation method and the degree of sulfation on the anticoagulant properties of dermatan sulfate derivatives

摘要: Abstract Six oversulfated dermatan sulfate (DS) derivatives, differing in their tissue origin (porcine skin, bovine and porcine intestinal mucosa), the oversulfation method of preparation, have been tested for anticoagulant properties. In first method, SO3-trimethylamine complex is added to a DS sodium salt dissolved formamide while it DS-benzethonium dimethyl second method. The rate sulfation these compounds ranged from 7.8 11.5 percent sulfur on weight basis, whereas 6% 12% natural heparin respectively. potency was assessed by determining catalytic effect each glycosaminoglycan inhibition thrombin (i) plasma (ii) purified cofactor II(HC II) or (iii) antithrombin III(AT III). Factor Xa presence AT III has also investigated. increased found enhance activity native whatever used, could be catalysed only most sulfated derivative obtained two derivatives which were less oversulfated, exhibit equal even higher effects when compared four other derivatives. use provides slightly strong properties may constitute effective antithrombotic drugs with no bleeding tendency, side perhaps related high sulfation.