含RGD多肽以及衍生物的舒血管作用

含RGD多肽以及衍生物的舒血管作用

迪丽努尔, 赵明, 彭师奇^*, 唐朝枢, 周琴璐, 李强

1. 北京医科大学药学院, 北京 100083;
2. 北京市体育科学研究所, 北京 100050

收稿日期:1996-03-11 修回日期:1996-09-23 出版日期:1997-03-15 发布日期:1997-03-15
通讯作者: 彭师奇*

Vasodilation Effects of RGD Containing Peptides and Derivatives

Dilinuer Shabituove, Ming Zhao, Shi-Qi Peng^*, Chao-Shu Tang, Qin-Lu Zhou, Qiang Li

1. School of Pharmaceutical Sciences; Beijing Medical University; Beijing 100083;
2. Beijing Research Institute of Sports Sciences; Beijing 100050

Received:1996-03-11 Revised:1996-09-23 Online:1997-03-15 Published:1997-03-15
Contact: Shi-Qi Peng*

摘要/Abstract

摘要： 已经证实纤维蛋白分子内两个区域内的氨基酸序列可以介导纤维蛋白与GPIIb/II-Ia受体的结合。除单克隆抗体外, 用合成的含RGD和APLRV的小分子多肽可以封闭GPIIb/II-Ia的这种结合功能, 我们的初步研究发现, RGDS除具有抑制血小板聚集和抗血栓形成的作用外, 还显示舒血管作用。为了证实RGDS相关多肽的舒血管作用, 研究了RGDF, APLRV, APLRVRGDS, APLRVRGDF, 在体外用NE预处理大鼠的动脉肌条后观察了上述合成多肽的舒血管作用, 检测了三种剂量(10^-5 mol/L, 10^-6 mol/L, 10^-7 mol/L)下收缩的肌条舒张的程度。

关键词: RGD序列, APLRV, 舒血管作用

Abstract: The binding of Fgn to GPIIb/IIIa has confirmed that there are two distinct amino acid sequences within the Fgn molecule that are responsible for mediating its attachment to GPIIb/IIIa receptor. In addition to monoclonal antibodies, the binding function of GPIIb/IIIa can be blocked by synthetic small peptides containing the RGD and APLRV sequence. In our preliminary study it was found that besides inhibition of platelet aggregation and thrombus formation RGDS showed vasodilation effects as well. In an attempt to confirm the vasodilation effect of RGDS related peptides, RGDF, APLRV, APLRVRGDS and APLRVRGDF were investigated. The effects of these synthetic peptides on rat aortic strips pretreated with NE in vitro were observed. The relaxing extents of contracted strips for the peptides at three doses (10^-5 mol/L, 10^-6 mol/L, 10^-7 mol/L) were recorded.

Key words: RGD Sequeence, APLRV, Vasodilation

Supporting: This Project was supported by the National Natural Science Foundation of China.

迪丽努尔, 赵明, 彭师奇^*, 唐朝枢, 周琴璐, 李强. 含RGD多肽以及衍生物的舒血管作用[J]. .

Dilinuer Shabituove, Ming Zhao, Shi-Qi Peng^*, Chao-Shu Tang, Qin-Lu Zhou, Qiang Li. Vasodilation Effects of RGD Containing Peptides and Derivatives[J]. .