Fucosylated chondroitin sulfate (FCS), an unusual glycosaminoglycan with fucose side chains, is a promising anticoagulant agent. To assess the effect of its structure on anticoagulant activity, its derivatives with various degrees of fucosylation (DF), molecular weights (Mw) and sulfation patterns were prepared and characterized. Biological tests showed that their APTT (activated partial thromboplastin time) prolonging activity and intrinsic factor Xase complex (factor IXa-VIIIa-Ca²⁺-PL complex) inhibitory activity were both reduced in FCS derivatives with lower Mw and DF. However, FCSs with DF at least 16% resulted in greater heparin cofactor II (HCII)-dependent thrombin inhibitory activity in response to decreasing DF, and these activities did not depend on Mw (Mw > 5.2 kDa). Solution competition binding assay further suggested that modulating the DF of FCS derivatives might enhance inhibition of thrombin by activating HCII. These findings imply that FCS derivatives with suitable chain length and DF value may be novel anticoagulants by activating HCII.

岩藻糖基化硫酸软骨素（FCS）是一种有前途的抗凝血剂，它是一种具有岩藻糖侧链的不寻常的糖胺聚糖。为了评估其结构对抗凝活性的影响，制备并表征了具有不同岩藻糖基化度（DF），分子量（Mw）和硫酸化模式的衍生物。生物学测试表明，它们的APTT（活化的部分凝血活酶时间）延长活性，内在因子Xase复合物（因子IXa-VIIIa-Ca ²⁺-PL复合物的抑制活性在Mw和DF较低的FCS衍生物中均降低。但是，DF含量至少为16％的FCS会响应于DF含量降低而产生更大的肝素辅因子II（HCII）依赖性凝血酶抑制活性，并且这些活性不依赖于Mw（Mw> 5.2 kDa）。溶液竞争结合试验进一步表明，调节FCS衍生物的DF可能通过激活HCII增强对凝血酶的抑制作用。这些发现暗示具有合适链长和DF值的FCS衍生物可能是通过激活HCII的新型抗凝剂。