Spiramine N-6的抗血小板活性研究

A Study of Anti-platelet Activity of Spiramine N-6

采用Ｂｏｒｎ氏比浊法观察了ｓｐｉｒａｍｉｎｅＮ－６在体外和体内对兔血小板聚集功能的影响．应用荧光分光光度法测定其对血小板５－ＨＴ释放反应的作用．结果：ｓｐｉｒａｍｉｎｅＮ－６在体外选择性抑制血小板活化因子（ＰＡＦ）诱导的血小板聚集，并呈量效关系，其ＩＣ５０＝２６μｍｏｌ／Ｌ；２ｍｇ／ｋｇｓｐｉｒａｍｉｎｅＮ－６静注后明显抑制ＰＡＦ和花生四烯酸（ＡＡ）诱导的血小板聚集，最大抑制率于给药后６０，３０ｍｉｎ分别为（５０４±４４）％和（７７３±３３）％（与生理盐水组对照Ｐ＜００５）；ｓｐｉｒａｍｉｎｅＮ－６呈浓度依赖性减少ＰＡＦ和ＡＡ引起血小板５－ＨＴ的释放，其ＩＣ５０分别为３３５ｕｍｏｌ／Ｌ和６４７μｍｏｌ／Ｌ．结果表明ｓｐｉｒａｍｉｎｅＮ－６是一种较强的抗血小板聚集剂．

Born's method was used to study the effects of spiramine N-6 on rabbit platelet aggregation in vitro or in vivo. With fluorophotometry, influence of spiramine N-6 on 5-HT release from platelets was observed. The results showed that in vitro spiramine N-6 selectively inhibited platelet-activating factor (PAF)-induced platelet aggregation in concentration-dependant manner, with IC 50 =26 μmol/L; spiramine N-6 2 mg/kg iv significantly suppressed PAF- or arachidonic acid (AA)-induced aggregation, with the maximal inhibitory rate (50 4±4 4) % or(77 3±3 3)% at 60 or 30 min after iv respectively. Spiramine N-6 concentration-dependant decreased platelet 5-HT release stimulated by PAF or AA, with the IC 50 value of 33 5 μmol/L or 54 7 μmol/L respectively. The results demonstrated that spiramine N-6 is a comparatively potent anti-platelet agent.