【摘 要】
：
阿司匹林耐药或无感应严重降低了阿司匹林的治疗作用。为了克服这个问题,将四肽RGDV以共价键的方式与阿司匹林结合,得到具有血栓靶向性的小分子结构：阿司匹林-RGDV(A-RGDV
【机 构】
：
首都医科大学化学生物学与药学院,北京市,100069
论文部分内容阅读
阿司匹林耐药或无感应严重降低了阿司匹林的治疗作用。为了克服这个问题,将四肽RGDV以共价键的方式与阿司匹林结合,得到具有血栓靶向性的小分子结构：阿司匹林-RGDV(A-RGDV)。通过二维核磁与质谱确定了A-RGDV的四聚体结构。利用透射电子显微镜观察到四聚体在水中自组装为5-50 nm直径的纳米颗粒。通过扫描电子显微镜与原子力显微镜观察到,大鼠血液中A-RGDV由较小的纳米结构组装为更大更稳定的颗粒。对药物分布的研究中发现大鼠血液中的A-RGDV可以保持结构完整性,直到血栓部位,释放出阿司匹林。体外抗血小板聚集试验证实A-RGDV可以选择性的抑制花生四烯酸引起的血小板聚集。这个过程包括释放阿司匹林、作用于环氧合酶以及降低GP Ⅱ b/Ⅲa的表达。体内试验中,A-RGDV的抗栓有效剂量比阿司匹林剂量低16-700倍。
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