阿魏酸衍生物高分子药物的合成及其对血小板聚集和对TXB_2,6-Keto-PGF_(1α)释放的影响  

Synthesis of the Polymeric Drug,a Derivative of Ferulic Acidand Its Effect on Platelet Aggregation andRelease of TXB\-2 and 6KetoPGF1

作　　者：李天锡[1,2] 袁才英 杨俊旺 单春文[1,2] 

机构地区：[1]兰州医学院药学系药物化学教研室 [2]解放军兰州医学高等专科学校药理教研室

出　　处：《中国药物化学杂志》1999年第2期98-101,共4页Chinese Journal of Medicinal Chemistry

摘　　要：以吲哚美辛（１）为原料先经酯化反应和Ｋｎｏｅｖｅｎａｇｅｌ缩合，再与可溶性淀粉连接，合成了侧链含有阿魏酸的高分子载体药物（４），该化合物未见文献报道．用比浊法和放免法测定了（４）体外对兔血小板聚集以及对ＴＸＢ２，６ＫｅｔｏＰＧＦ１α含量的影响．化合物（４）２４０μｍｏｌ·Ｌ－１对ＡＡ诱导的兔血小板聚集的抑制率为３９６％，对ＴＸＢ２释放的抑制率为２８７％．与吲哚美辛（１）或阿魏酸比较，阿魏酸衍生物高分子载体药物（４）显示有抑制兔体外血小板聚集和抑制ＴＸＢ２，６ＫｅｔｏＰＧＦ１α释放的作用，呈现明显的药物协同作用．The polymeric drug(FAIS) which contains ferulic acid(FA) was synthesized from indomethacin via esterfication and the Knoevenagel condensation,and then conjunction with soluble starch(S).This new compound was obtained for the first time.The results of preliminary pharmacological tests showed that the FAIS could inhibit the rabbit platelet aggregation induced by arachidonic acid(AA) and release of TXB2 and 6KetoPGF1.Its activity was stronger than that of FA and indomethacin.It was in evidence to express the good synergic effect.

关 键 词：阿魏酸 吲哚美辛 高分子载体 血小板聚集 

分 类 号：TQ464.9[化学工程—制药化工] R973.2[医药卫生—药品]