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藜芦生物碱抗血栓作用及构效关系研究 被引量:9

Study on Antithrombotic Activities and Structure-activity Relationships of Veratrum nigrum Alkaloids
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摘要 目的:研究藜芦总生物碱(Vn A)以及6种单一生物碱(A1-A6)的抗血栓活性及作用机制。方法:测定Vn A以及A1-A6对大鼠下腔静脉血栓、凝血参数(APTT、PT、TT)、ADP及凝血酶诱导的兔血小板聚集的影响。结果:Vn A、A1-A5能显著降低血栓湿质量和血小板聚集率,延长TT,对APTT和PT无明显影响。A6对所测指标均无明显影响。结论:Vn A以及A1-A5有抗血栓活性,A6无抗血栓活性。A2可能是藜芦生物碱抗血栓活性的主要有效成分。抗血栓作用与抗血小板聚集以及TT的延长有关。西藜芦碱骨架是抗血栓活性必需的,C3位的酯基取代能增强抗血栓活性。 Objective: To explore antithrombotic effects and mechanisms of total alkaloids( Vn A) and single alkaloids( A1 - A6)from Veratrum nigrum. Methods: The effects of Vn A and A1 - A6 on thrombosis and coagulation parameters( APTT,PT and TT) were examined in rat in vivo,while their effects on platelet aggregation induced by ADP and thrombin were determined in rabbit in vitro. Results: Vn A and A1 - A5 decreased thrombus wet weight and platelet aggregation,increased TT,while they had no influence on APTT or PT. A6 had no obvious effect on thrombus wet weight,platelet aggregation or coagulation parameters. Conclusions: Vn A and A1- A5 have antithrombotic activities on venous thrombosis. The effective component in Vn A is A2 probably. The antithrombotic effects are possibly related to the inhibition of platelet aggregation and the extension of TT. The cevanine type skeleton of steroidal alkaloids is necessary for antithrombotic activities and the ester substitute at C3 can enhance antithrombotic activities.
出处 《中药材》 CAS CSCD 北大核心 2014年第11期2034-2038,共5页 Journal of Chinese Medicinal Materials
基金 国家自然科学基金面上项目(20872011)
关键词 抗凝 抗血小板 抗血栓 甾体生物碱 藜芦 Anticoagulation Antiplatelet Antithrombotic Steroidal alkaloids Veratrum nigrum L.
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