摘要
目的研究六肽对人血小板聚集率的影响。方法采集健康受试志愿者肘前静脉血，以构橼酸钠抗凝，分为空白对照组、六肽（终浓度1×10^-6～1×10^-5mol·L-1）五个浓度受试药物组，以及依替巴肽（1×10^-6mol·L-1）、氯吡格雷（3×10^-5mol·L-1）、双嘧达莫（2×10^-6mol·L-1）和阿司匹林（2．8×10^-4mol·L-1）4个阳性对照组，每组6例，分别以二磷酸腺苷（ADP）＋肾上腺素（NE）、花生四烯酸（AA）和凝血酶为诱导剂，比浊法测定人血小板在不同诱导剂诱导时的血小板聚集率。结果1×10^-6mol·L-1六肽组对ADP、AA和凝血酶诱导的血小板聚集的抑制率分别为（98．81±2．25）％、（94．58±0．73）％和（33．46±5．56）％，显著高于空白对照组（P〈0．01）。在ADP诱导时，1×10^-6mol·L-1六肽的抗血小板聚集活性显著高于阳性对照药物氯吡格雷、双嘧达莫和阿司匹林（P〈0．01）。六肽在ADP、AA和凝血酶诱导的人血小板的IC50分别为8．91×10^-8mol·L-1、9．33×10^-8mol·L-1和4．17×10^-6mol·L-1，依替巴肽的IC50为1．00×10^-7mol·L-1。结论六肽在体外具有抑制人血小板聚集的作用。
AIM This study aimed to investigate the anti- aggregation effects of hexapeptide on human platelets. METHODS Venous blood of healthy volunteer was taken, and was made into anticoagulation blood with sodium citrate, divided into control group, hexapeptide groups （1 ×10^-9 - 1 ×10^-5 mol L-1） and four kinds of positive groups, including clopidogrel group （3 ×10^-5 mol.L-1）, dipyridamole group （2 ×10^-4 mol＇L-1）, aspirin group （2.8 ×10^-4 mol L-1） and eptifibatide group （1 ×10^-4 mol L-1）. Each group included 6 samples. The inducers were adenosine diphosphate （ADP） ＋ adrenalin, arachidonic acid and thrombin, respectively. The human platelet aggregation rates induced by different inducers were determined with the method of turbidimetry. RESULTS The aggregation inhibition rates of 1 ×10^-4 mol.L-1 hexapeptide in human induced by ADP, araehidonic acid and thrombin, were （98.81 ± 2.25）%, （94.58 ± 0.73）% and （33.46 ± 5.56）% respectively, and which were all significant higher than the control group （P 〈 0.01）. Induced by ADP, the anti-platelet aggregation activity of 1 ×10^-6 mol. L-1 hexapeptide was significant higher than that of clopidogrel, dipyridamole or aspirin （P 〈 0.01 ）, but had no different with eptifibatide （P 〉 0.05）. The anti-aggregation IC50 of hexapeptide of ADP, arachidonic acid and thrombin, were 8.91 ×10^-8 mol.L-l, 9.33 ×10^-8 mol.L-1 and 4.17×10^-6 mol .L-1, respeetively. The anti-aggregation IC50 of eptifibatide indueed by ADP was 1.00 ×10^-7 mol .L-1. CONCLUSION Hexapeptide has the effect of anti-platelet aggregation in human in vitro.
出处
《中国新药与临床杂志》
CAS
CSCD
北大核心
2013年第4期315-318,共4页
Chinese Journal of New Drugs and Clinical Remedies
基金
陕西省教育厅项目(11JK0722)
西安医学院附属医院项目(XYFY11-02)
关键词
六肽
血小板聚集
腺苷二磷酸
肾上腺素
凝血酶
hexapeptide
platelet aggregation
adenosine diphosphate
epinephrine
thrombin
