溶血栓肽(HPA)的合成及其生物活性研究

THE STUDY ON SYNTHESIS AND BIOACTIVITY OF DISSOLVING THROMBUS PEPTIDE (HPA)

采用多肽固相合成法合成了序列为GPRVVE并带有一个茴香醚修饰基团的六肽(HPA),经HPLC检测,其纯度达96.7％,氨基酸组成及分子量测定结果均与预期结果相符合。当家兔静脉注射HPA剂量达180μg/kg时,血小板血栓形成被抑制约32％,并可使家兔血浆优球蛋白溶解时间平均缩短100分钟。用平板法测定,HPA对人纤维蛋白聚合物具有一定的解聚作用,并与尿激酶有显著的协同效应。

A hexyl peptide, GPRVVE, modified with anisole (HPA) was synthesized by using the solid phase peptide synthesis. The purified peptide was judged to be 96. 7%pure on HPLC. The data obtained from amino acid analysis and fast atom bombimg mass spectrum were in good agreement with theoretical values. The formation of thrombus was decreased by 32%and time for dissolving of euglobulin was shortened by 100 min after treatment to rabbits with HPA (i. v. 180ug/kg WT). The action of HPA detected by flatbed method shows dissolving aggregation of fibrinogen significantly and possess the associate action with urokinase.