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红花黄酮成分抑制血小板激活因子介导的血小板活化作用

INHIBITORY EFFECT OF FLAVONOLS OF CARTHAMUS TINCTORIUS L. AGAINST RABBIT PLATELET ACTIVATION INDUCED BY PLATELET ACTIVATING FACTOR

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【作者】 陈文梅; 金鸣; 吴伟; 李金荣; 臧宝霞; 朴永哲;

【Author】 CHEN Wen mei, JIN Ming, WU Wei, LI Jin rong, ZANG Bao xia, PIAO Yong zhe (Beijing Institute of Heart, Lung and Blood Vessel Diseases, Beijing 100029, China)

【机构】 北京市心肺血管疾病研究所药理研究室; 北京市心肺血管疾病研究所药理研究室 北京100029; 北京100029; 北京10;

【摘要】 目的 观察红花黄酮成分杨梅素 (Myr)和山奈酚 (Kae)对血小板激活因子 (PAF)诱导的兔洗涤血小板聚集、5 HT释放及血小板内游离钙离子浓度升高的影响。方法 以比浊法测定家兔洗涤血小板 (WRP)聚集 ,邻苯二甲醛 (OPT)荧光法测定 5 HT浓度 ,Fura 2荧光探针测定血小板内游离钙离子浓度。结果 Myr和Kae体外呈浓度依赖性地抑制PAF诱发的WRP聚集及 5 HT释放。Myr抑制WRP聚集的IC50 为 17 5 μmol·L- 1 ;抑制 5 HT释放的IC50 为6 4 1μmol·L- 1 。Kae抑制聚集、释放作用的IC50 分别为 73 7μmol·L- 1 和 12 8μmol·L- 1 ;同时Myr和Kae均能明显抑制PAF引起的血小板内游离钙增高。结论 Myr和Kae可抑制PAF诱导的血小板活化作用

【Abstract】 AIM To observe the inhibitory effect of myricetin (Myr) and kaempferol (Kae) (components of Carthamus tinctorius L.) against washed rabbit platelet (WRP) aggregation, 5 HT release and intercellular free calcium concentration elevation induced by platelet activating factor (PAF). METHODS The platelet aggregation induced by PAF was determined with turbidity assay. The platelet 5 HT release and platelet inner free calcium concentration elevation induced by PAF were measured by OPT fluorescence assay and Fura 2/AM probe fluorescent technique respectively. RESULTS The WRP aggregation and 5 HT release induced by PAF (9 55×10 -9 mol·L -1 ) were both inhibited by Myr and Kae in a concentration dependent manner. WRP aggregation rate can be significantly decreased by Myr and Kae. Low concentration Kae (21 8 μmol·L -1 ) showed no inhibition effect against platelet aggregation. The IC 50 of Myr and Kae against WRP aggregation were 17 5 μmol·L -1 and 73 7 μmol·L -1 respectively. It was shown by OPT fluorescence assay that Myr (7 86 μmol·L -1 ) and Kae (21 8 μmol·L -1 ) were not effective against platelet 5 HT release ( P >0 05). The IC 50 of Myr was 64 1 μmol·L -1 and that of Kae was 128 μmol·L -1 . It was also found that the platelet inner free calcium concentration elevation evoked by PAF (4 78×10 -10 mol·L -1 ) was inhibited by Myr and Kae. CONCLUSION The rabbit platelet activation induced by platelet activating factor can be inhibited by Myr and Kae.

【基金】 国家自然科学基金 ( 396 70 884) ;北京市自然科学基金 ( 70 130 34) ;北京市跨世纪科技人才工程;北京市高科技实验室课题资助项目
  • 【文献出处】 药学学报 ,Acta Pharmaceutica Sinica , 编辑部邮箱 ,2001年12期
  • 【分类号】R285
  • 【被引频次】93
  • 【下载频次】378
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