鱿鱼墨多糖的硫酸酯化及抗凝血活性

Sulfation of a Squid Ink Polysaccharide and Its Anticoagulant Activities

采用三氧化硫吡啶-二甲亚砜体系对北太平洋鱿鱼墨多糖(SIP)及其三乙胺盐进行硫酸酯化.对硫酸酯化后多糖的基本成分分析表明,硫酸酯化对鱿鱼墨多糖的单糖组成影响不大,但是分子量降低,硫酸酯化后,糖单元数:硫酸基的摩尔比约为3:2.采用红外光谱和一维核磁技术对硫酸酯化后多糖的结构进行了分析,结果表明,硫酸酯化主要发生在N-乙酰半乳糖胺(GalNAc)的4,6位上.进一步的凝血活性分析表明,它具有较好的延长活化部分凝血活酶时间(APTT)和凝血酶原时间(PT)的效果.凝血因子抑制实验则表明,硫酸酯化后的鱿鱼墨多糖(TBA-1)对凝血因子FⅡa和FⅩa均有显著的抑制作用.

This paper firstly reported the preparation,characterization,and anticoagulant activities of a chemically sulfated polysaccharide isolated from the ink of the squid,Ommastrephes bartrami.The squid ink polysaccharide（SIP） with an unique of trisaccharide repeat ■3GlcAβ1-4（GalNAcα1-3）Fucα1■nwas sulfated with the pyridine-sulfur-trioxide complex in dimethyl sulfoxide（DMSO） under different conditions.Chemical composition analysis of the sulfated SIPs indicated that the sulfation had no obvious effect on the monosaccharide composition of the polysaccharides but decreased the molecular weight,the molar ratio of monosaccharide unit to sulfate was about 3：2.Structural characterization of sulfated SIPs using IR and NMR spectra indicated that sulfation mainly occurred at the 4,6-position of GalNAc,so the main structure of the sulfated SIPs were clearly identified as ■3GlcAβ1-4（4,6-SO4-GalNAcα1-3）-Fucα1■n.Anticoagulant activity assay of the sulfated SIPs（TBA-1 and DMSO-1） showed they have no obvious effect on TT,but prolong PT and APTT.The effects of TBA-1 on inhibition of thrombin（FⅡa） and FⅩa activities mediated by antithrombin Ⅲ or heparin cofactor Ⅱ were also examined in vitro.The results reveale TBA-1 inhibited both the activities of FⅡa and FⅩa obviously.Thus,our results indicate that sulfate SIP is a potential candidate for the prevention of blood coagulant.