化学修饰对组织型纤溶酶原激活剂的纤溶活性和体内半衰期的影响  

Effects of Chemical Modification on the Fibrinolytic Activity and Half- Life of Recombinant Tissue-Type Plasminogen Activator

作　　者：吴本传[1] 刘红[1] 陈昭烈[1] 黄培堂[1] 

机构地区：[1]军事医学科学院生物工程研究所,北京100071

出　　处：《药物生物技术》2003年第6期368-371,共4页Pharmaceutical Biotechnology

基　　金：国家"863"基金资助项目(Z18-03-12)

摘　　要：用肝素、右旋糖酐和聚乙二醇对重组组织型纤溶酶原激活剂(rt-PA)进行化学修饰。不同的化学修饰物对rt-PA体外纤维蛋白溶解活性的影响不同。肝素修饰rt-PA的纤维蛋白溶解活性提高63％;右旋糖酐和聚乙二醇修饰rt-PA的纤维蛋白溶解活性则分别降低了36％和63％。rt-PA经化学修饰后半衰期均有所延长,其中聚乙醇修饰的rt-PA的半衰期由修饰前的3.4 min延长至6.3 min。Chemical modification of surface amino groups of recombinant tissue-type plasminogen activator (rt-PA) with heparin, polyethylene glycol (PEG) and dextran was conducted. It was found that heparin modification of rt-PA resulted in 63% increase of fibrinolytic activity. However, the fibrinolytic activity of rt-PA modified with PEG and dextran decreased 63% and 36% , respectively. Modification of rt-PA with heparin, PEG and dextran prolonged the half-life of rt-PA to a different degree, the half-life of rt-PA modified with PEG prolonged from 3.4 min of untreated rt-PA to 6.3 min.

关 键 词：重组组织型纤溶酶原激活剂 化学修饰 纤维蛋白溶解活性 半衰期 

分 类 号：Q55[生物学—生物化学]