Journal article
Modulating the degree of fucosylation of fucosylated chondroitin sulfate enhances heparin cofactor II-dependent thrombin inhibition
European Journal of Medicinal Chemistry, Vol.154, pp.133-143
2018
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Source: InCites
Abstract
<p>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-Ca<sup>2</sup>+-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.</p>
Details
- Title
- Modulating the degree of fucosylation of fucosylated chondroitin sulfate enhances heparin cofactor II-dependent thrombin inhibition
- Creators
- Li Xu - Chinese Academy of Sciences, ChinaChuang Xiao - Chinese Academy of Sciences, ChinaSteven W Purcell - Southern Cross UniversityMingyi Wu - Chinese Academy of Sciences, ChinaJinhua Zhao - Chinese Academy of Sciences, ChinaLisha Lin - Chinese Academy of Sciences, China
- Publication Details
- European Journal of Medicinal Chemistry, Vol.154, pp.133-143
- Identifiers
- 4534; 991012821355602368
- Academic Unit
- National Marine Science Centre; School of Environment, Science and Engineering; Marine Ecology Research Centre; Faculty of Science and Engineering
- Resource Type
- Journal article