β-1,4-葡聚糖硫酸酯的制备及其抗凝血活性  

Preparation and Anticoagulation Activity of β-1,4-Glucan Sulfate

作　　者：王兆梅[1] 李琳[1] 郭祀远[1] 肖凯军[1] 

机构地区：[1]华南理工大学轻化工研究所,广东广州510640

出　　处：《林产化学与工业》2006年第4期1-5,共5页Chemistry and Industry of Forest Products

基　　金：国家自然科学基金资助项目(20436020);广东省自然科学基金资助项目(000453)

摘　　要：对微晶纤维素(MCC)进行硫酸酯化修饰,得到多种β-1,4-葡聚糖硫酸酯(GS),其硫酸取代度(Ds)在1.10～1.70范围内.选择Ds为1.70的GS用于结构分析和抗凝血活性研究.IR分析表明,MCC通过硫酸化反应引入了硫酸酯基,13C NMR揭示,硫酸酯化主要发生在C6,部分在C2,而C3位不发生硫酸酯化反应.凝血分析表明,0.2 mg/L的GS即可显著延长血浆的活化凝血活酶时间(tAPTT)和凝血酶时间(tTT),使血浆tAPTT延长两倍,所需GS的剂量为0.7 mg/L,低于活性为150 IU/mg的肝素,在一定质量浓度范围内,GS的体外抗凝血活性与肝素相当.显色分析揭示,GS的抗凝血机制主要在于通过抗凝血酶AT-Ⅲ的调节作用抑制凝血因子Ⅱa和Xa的活性.Various β-1,4-glucan sulfates(GS) were synthesized by sulfate of microcrystalline cellulose. Their sulfate substitute degree (D_s) varied in the range of 1.10 to 1.70. GS with D_s of 1.70 was selected for structural analysis and anticoagulation investigation. IR spectra showed the introduction of sulfate groups by sulfation. ~ 13 C NMR indicated that sulfation occurred mainly at C_6, partially at C_2 and no sulfate substitution occurred at C_3. Coagulation assays showed that 0.2mg/L GS could significantly prolong t_ APTT and t_ TT in plasma. The dosage of GS required to double t_ APTT of normal human plasma was 0.7mg/L , lower than that of heparin with the anticoagulation activity of 150IU/mg . Its potent of anticoagulation in vitro reached the efficacy of heparin in definite range of concentration. Chromogenic analysis revealed that the anticoagulation mechanism of GS was mainly due to the inhibition of the coagulation factors Ⅱa & Xa activities mediated by antithrombin AT-Ⅲ.

关 键 词：葡聚糖硫酸酯 抗凝血 机制 

分 类 号：TQ35[化学工程] O614[理学—无机化学]