摘要: |
甲壳质及壳聚糖的硫酸酯化反应是其化学修饰中最吸引人的研究内容之一。由于它们与肝素有相似骨架, 经硫酸酯化,引入-NHSO3H, - CH2OSO3H - OSO3H, COOH,-CH2COOH基团后得到甲壳质(壳聚糖)类肝素药物,显示出抗栓、抗凝血性能(李鹏程等,1998;曾宪放等,1992;Proeyanat et al.,2002);如Muzzarelli(1985)早已预见并证实其抗凝血活性;莫斯科血液研究中心病理药理系止血组的研究人员也证明了壳聚糖硫酸酯具有抗凝血活性,他们将肝素与壳聚糖硫酸酯以1∶1的比例给家兔静脉注射各0.5mg/kg,与单纯用肝素1mg/kg对照组比较,其抗凝血效应基本接近,但对照组有出血副作用,而试验组无副作用,可以证明壳聚糖硫酸酯具有既抗凝血又止血的双重调节作用;Tokura等(1994)证实分子质量大小和脱乙酰度不同对磺化产物的抗凝血活力有影响,样品分子质量26000 Da的活性最高,脱乙酰度70%比45%的抗凝血活性更强,脱乙酰度为95%的壳聚糖磺化后抗凝血活性最弱。在中国这方面的研究相对较少,特别是分子中含硫的多寡对生物活性的影响还未见报道。本文作者就壳聚糖的磺化产物对大鼠抗栓、抗凝血进行了研究,表明壳聚糖硫酸酯具有一定的抗栓、抗凝血效果,且具有一定的量效关系,这对今后该方面的进一步研究提供了科学理论依据。 |
关键词: 壳聚糖 血栓 凝血时间 |
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基金项目:中国科学院知识创新工程方向性课题和青岛市科技项目联合资助 |
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Effect of Chitosan Sulfate on Thrombus Formation and Cruor Time in Mice |
XING Ronge1, LIU Song1, YU Huahua1, LI Zhien2, LI Pengcheng2
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1.Institute of Oceanology, The Chinese Academy of Sciences;2.Graduate School, Chinese Academy of Sciences
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Abstract: |
Two sulfated chitosan derivatives were prepared in this paper (CSA and CSB that is low and high replacement) and their medical effect was researched. Aim: to study the effect of chitosan derivatives on thrombus formation and cruor time in mice. Method: sixty mice were divided in to six groups and each group was raised with chitosan derivatives (CSA、CSB) 200 and 600mg /kg, aspirin 10 mg /kg, and 0.5% sodium carboxymethyl cellulose 2 ml /mice respectively. The levels of thrombus formation and cruor time were calculated in mice. Conclusion: two kinds of sulfated chitosan of the different sulfur con tent had been successfully prepared, that is CSA:DD 21.23%;CSB:DD 42.21%.Their yields are all over 90%;CSA、CSB at doses of 200mg /kg barely in fluence the rate of thrombus formation and cruor time, however, CSB at doses of 600 mg /kg significantly decreased the weight of thrombus and increased cruor time in
mice: decreasing 14.21% thrombus weight and increasing 14.31% cruor time. |
Key words: chitosan thrombus formation cruor time |