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新型磺酰胺类化合物SZ427的抗血小板聚集作用

Effect of newsulfonamide compounds SZ427 on antiplatelet aggregation

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【作者】 郑佳莉应珂许丽萍赵剑刘铮

【Author】 ZHENG Jia-li;YING Ke;XU Li-ping;ZHAO Jian;LIU Zheng;School of Life Science and Biopharmaceutics,Shenyang Pharmaceutical University;

【机构】 沈阳药科大学生命科学与生物制药学院

【摘要】 目的研究新型磺酰胺类化合物4-乙氧基-N,N’-二(4-吡啶乙基)-1,3-苯二磺酰胺(SZ427)的抗血小板聚集作用。方法在体外药效学实验中,采用血小板聚集分析仪观察化合物SZ427对花生四烯酸(arachidonic acid,AA)、二磷酸腺苷(adenonisine disphosphate,ADP)和胶原诱导的家兔血小板聚集的影响。在体内药效学实验中,通过小鼠尾静脉出血时间、大鼠颈总动脉血栓和小鼠急性肺血栓三种模型分别观察化合物SZ427对出血时间、血栓质量和死亡时间的影响。结果在体外药效实验中,化合物SZ427能显著抑制AA、ADP和胶原诱导的家兔血小板的聚集作用;在体内药效学实验中,化合物SZ427能延长小鼠尾静脉出血时间,具有抗血小板聚集作用;能减少大鼠颈总动脉血栓质量,抑制血栓形成;能显著延长急性肺血栓小鼠的死亡时间,明显降低死亡率。结论化合物SZ427能抑制慢性血栓和急性血栓的形成,具有抗血小板聚集的作用。

【Abstract】 Objective To assess the effects of antiplatelet aggregation of SZ427. Methods In vitro the antiplatelet aggregation activities of SZ427 against arachidonic acid( AA),adenosine diphosphate( ADP) and collagen were evaluated by platelet aggregation analyzer;in vivo,tail vein bleeding time of mice,rat carotid artery thrombosis,acute pulmonary thrombosis in mice were designed to evaluate the function. Results In vitro the SZ427 can significantly inhibit ADP,AA,and collagen-induced platelet aggregation; in vivo,the SZ427 is capable to prolong tail bleeding time of mice and have the effect of antiplatelet aggregation;Decrease the weight of thrombus in rat,inhibit the formation of blood clots;extend the death time and lower the death rate of acute pulmonary thrombosis in mice. Conclusions SZ427 can inhibit the formation of chronic-and acute-thrombosis,plays a role in antiplatelet aggregation.

  • 【文献出处】 沈阳药科大学学报 ,Journal of Shenyang Pharmaceutical University , 编辑部邮箱 ,2017年02期
  • 【分类号】R96
  • 【下载频次】170
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