Inhibitory effects of copper-aspirin complex on platelet aggregation  

作　　者：沈志强[1,2] 陈植和[1,2] 马国义 王德成 吴婉玲[1,2] 刘伟平 杨一昆 熊惠周 

机构地区：[1]云南省天然药物药理重点实验室 [2]昆明医学院

出　　处：《中国药理学报》1997年第4期358-362,共5页Acta Pharmacologica Sinica

摘　　要：目的：研究阿司匹林铜（ＣｕＡｓｐ）对血小板聚集性的影响及其机制．方法：用Ｂｏｒｎ氏法测定ＣｕＡｓｐ对兔血小板聚集性的影响．用荧光光度法和放射免疫法观察ＣｕＡｓｐ对兔血小板５羟色胺的释放和ＴＸＢ２的产生及血浆中ＴＸＢ２和６ｋｅｔｏＰＧＦ１α水平的影响．结果：ＣｕＡｓｐ体外呈浓度依赖性抑制花生四烯酸（ＡＡ）诱导的血小板聚集和５羟色胺的释放（ＩＣ５０分别为１７和１９μｍｏｌ·Ｌ－１，９５％可信限为９－３３和１０－３０μｍｏｌ·Ｌ－１），且抑制ＴＸＢ２的产生（Ｐ＜００５）．ＣｕＡｓｐ１０ｍｇ·ｋｇ－１灌胃选择性抑制ＡＡ诱导聚集．降低血浆ＴＸＢ２，同时升高６ｋｅｔｏＰＧＦ１α的水平（Ｐ＜００５）．结论：ＣｕＡｓｐ体内外均有比Ａｓｐ更强的抗血小板聚集作用．IM: To study the inhibitory effects of copper aspirin complex (CuAsp) on platelet aggregation. METHODS: With adenosine diphosphate the effects of CuAsp on platelet aggregation in vitro or in vivo were investigated. Radioimmunoassay and fluoro￣photometry were used to measure throm￣box￣ane B 2 (TXB 2) generation from platelets, the levels of TXB 2 and of 6 keto PGF 1α in plasma and the platelet serotonin release reaction. RESULTS: In vitro , CuAsp inhibited arachidonic acid (AA) induced aggregation (IC 50 =17 μmol·L -1 , 95 % confidence limits: 9-33 μmol·L -1 ), the release of 5 HT (IC 50 =19 μmol·L -1 , 95 % confidence limits: 10-30 μmol·L -1 ), and TXB 2 generation from platelets ( P <0 05). CuAsp 10 mg·kg -1 ig selectively inhibited AA induced aggregation, and increased the 6 keto PGF 1α concentration in plasma while decreased that of TXB 2. CONCLUSION: CuAsp, in vitro or in vivo , shows more potent inhibitory effects on AA induced aggregation than aspirin (Asp), related to the inhibition of platelet cyclooxygenase and the release of active substances from platelets.

关 键 词：铜 阿司匹林 血小板聚集 

分 类 号：R971.1[医药卫生—药品]