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作 者:李玲[1] 李民[2] 沈月毛[1] 陈植和[3] 杜秀宝[2] 郝小江[1]
机构地区:[1]中国科学院昆明植物研究所,昆明650204 [2]云南省天然药物药理重点实验室防化研究院,北京102205 [3]云南省天然药物药理重点实验室昆明医学院,昆明650031
出 处:《天然产物研究与开发》2002年第3期7-10,共4页Natural Product Research and Development
基 金:国家杰出青年基金资助项目 (No .3 95 2 5 0 2 5 ) ;云南省科委应用基础研究基金资助项目 (No .99C0 0 79M)
摘 要:采用Born氏比浊法观察华北绣线菊小叶变种中分离得到的总碱和 9个hetisine型C2 0 二萜生物碱及其衍生物体外对血小板活化因子 (PAF)、花生四烯酸 (AA)和二磷酸腺苷 (ADP)三种诱导剂引起的血小板聚集活性的影响 ,并初步探讨了构效关系。结果表明 ,华北绣线菊小叶变种中总碱对PAF和ADP诱导的血小板聚集均有明显的抑制作用 ;9个hetisine型C2 0 二萜生物碱中 ,有 8个显著抑制PAF诱导的血小板聚集 ,其活性与分子结构明显相关 ;此外 ,hetisine型生物碱及其衍生物对ADP诱导的血小板聚集亦有一定的抑制作用 ,但总碱及生物碱对AA诱导的聚集影响不明显。提示hetisine型C2 0 二萜生物碱具有抗血小板聚集活性。Born's method was used to determine the effects of basic fraction and nine hetisine type C 20 diterpene alkaloids isolated from Spiraea fritschiana var. parvifolia and its derivatives on platelet activating factor(PAF),arachidonic acid(AA)and adenosine diphosphate(ADP) induced rabbit platelet aggregation in vitro. The activity structure relationship was also discussed.The results showed that the basic fraction markedly inhibited PAF and ADP induced rabbit platelet aggregation.Eight of the hetisine type C 20 diterpene alkaloids in this study significantly inhibited rabbit platelet aggregation induced by PAF.The inhibition was correlated to their structures.Moreover,the tested compounds inhibited ADP induced aggregation,while neither the basic fraction nor the compounds had effects on AA induced aggregation.It was suggested that hetisine type diterpene alkaloids had antiplatelet aggregation activity.
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