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Modulating the degree of fucosylation of fucosylated chondroitin sulfate enhances heparin cofactor II-dependent thrombin inhibition
Xu, Li; Gao, Na; Xiao, Chuang; Lin, Lisha; Purcell, Steven W.; Wu, Mingyi; Zhao, Jinhua
2018
Source PublicationEUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
ISSN0223-5234
Volume154Pages:133-143
Abstract

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. (C) 2018 Elsevier Masson SAS. All rights reserved.

Indexed BySCI
Language英语
Document Type期刊论文
Identifierhttp://ir.kib.ac.cn/handle/151853/64728
Collection中国科学院昆明植物研究所
Recommended Citation
GB/T 7714
Xu, Li,Gao, Na,Xiao, Chuang,et al. Modulating the degree of fucosylation of fucosylated chondroitin sulfate enhances heparin cofactor II-dependent thrombin inhibition[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2018,154:133-143.
APA Xu, Li.,Gao, Na.,Xiao, Chuang.,Lin, Lisha.,Purcell, Steven W..,...&Zhao, Jinhua.(2018).Modulating the degree of fucosylation of fucosylated chondroitin sulfate enhances heparin cofactor II-dependent thrombin inhibition.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,154,133-143.
MLA Xu, Li,et al."Modulating the degree of fucosylation of fucosylated chondroitin sulfate enhances heparin cofactor II-dependent thrombin inhibition".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 154(2018):133-143.
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