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作 者:郭琰 周铭涛 龚吕东 钟承志 李婷 颜宏 张海元 吴德松 叶雨佳 张金艳[3] 崔涛 朱兆云 GUO Yan;ZHOU Ming-tao;GONG Li-dong;ZHONG Cheng-zhi;LI Ting;YAN Hong;ZHANG Hai-yuan;WU De-song;YE Yu-jia;ZHANG Jin-yan;CUI Tao;ZHU Zhao-yun(Yunnan Institute of Materia Medica/Yunnan Province Company Key Laboratory for TCM and Ethnic Drug of New Drug Creation,Kunming 650111,China;Laboratory of Molecular Cardiology,Department of Cardiology,The First Affiliated Hospital of Kunming Medical University,Kunming 650032,China;Institute of Basic Medical Sciences,Xiyuan Hospital,China Academy of Chinese Medical Sciences,Bejing 100091,China)
机构地区:[1]云南省药物研究所/云南省中药和民族药新药创制企业重点实验室,昆明650111 [2]昆明医科大学附一院心内科分/子生物学实验室,昆明650032 [3]中国中医科学院西苑医院基础研究室,北京100091
出 处:《中国新药杂志》2023年第18期1874-1881,共8页Chinese Journal of New Drugs
基 金:云南省重大科技专项资助项目(2019ZF016)。
摘 要:目的:评价三七创新新药全三七片的抗血小板聚集作用及其作用优势。方法:采用人富血小板血浆和洗涤血小板,检测全三七片对不同血小板激活剂诱导的血小板聚集率和Ca^(2+)浓度;采用大鼠富血小板血浆,对比全三七片和三七提取物对二磷酸腺苷(ADP)诱导的血小板聚集率;通过注射80%乙醇建立胃出血模型大鼠,考察全三七片与阿司匹林对便潜血的影响;通过小鼠凝血实验和大鼠凝血四项的检测,观察全三七片的止血作用。结果:全三七片可以剂量依赖性地抑制ADP、凝血酶、U46619、胶原、anti-CD9诱导的人血小板聚集率(均P<0.01)和Ca^(2+)释放(P<0.05或P<0.01);可以抑制ADP诱导的大鼠血小板聚集率(P<0.01),且作用明显优于传统三七提取物;全三七片以及与阿司匹林联合用药均可降低胃出血模型大鼠的便隐血等级(均P<0.05),而单用阿司匹林则未见显著性差异(P>0.05);全三七片还可显著缩短小鼠的凝血时间和大鼠的活化部分凝血活酶时间,具有一定的止血作用。结论:三七创新药物全三七片具有显著的抗血小板聚集作用,具有多途径、多靶点的作用特点,且因其出色的止血作用还可以降低出血风险,是一种安全、有效的抗血小板新药。Objective:To evaluate the anti-platelet aggregation effect and advantages of Quansanqi tablets(PSQ),an innovative new drug of Panax notoginseng.Methods:Human platelet-rich plasma and washed platelets were used to detect the platelet aggregation rate and calcium ion concentration induced by different platelet activators;rat platelet-rich plasma was used to compare the platelet aggregation rate induced by ADP in PSQ and Panax notoginseng extract;gastric bleeding model rats were established by injecting 80%ethanol to investigate the effects of PSQ and aspirin on fecal occult blood;the hemostatic effect of PSQ was observed by mouse and rat coagulation test.Results:PSQ could dose-dependently inhibit ADP,thrombin,U46619,collagen and reduce anti-CD9-induced human platelet aggregation rate(P<0.01)and Ca^(2+)release(P<0.05 or P<0.01);it could inhibit ADPinduced rat platelet aggregation rate(P<0.01),with significantly better effect than Panax notoginseng extract PSQ could reduce the fecal occult blood grade in gastric bleeding model rats(P<0.05),while aspirin could not(P>0.05);it could also significantly shorten the coagulation time in mice and APTT time in rats,indicating certain hemostatic effect.Conclusion:PSQ has significant anti-platelet aggregation effect through multiple ways with multiple action targets,and can also reduce the risk of bleeding because of its excellent hemostatic effect,which is a safe and effective new antiplatelet drug.
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