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目的:观察和比较益母草碱、丁香酰胍醇及丁香酸氨基醇酯类化合物抗血小板聚集活性及其与结构的关系。方法:以血小板聚集为指标并计算IC(50)以比较各样品的作用强度。结果:益母草碱(Ⅰ),化合物Ⅱ,Ⅲ和Ⅳ1,2均能对抗ADP诱导大鼠和兔的血小板聚集作用,其IC(50)分别为0.97,4.4,5.2,0.36和1.14mg/ml。所有化合物在体外均有抑制ADP诱导大鼠和兔的血小板聚集的作用,以Ⅳ1,Ⅴ1和Ⅶ1,2的作用最强,IC(50)在0.15~0.36mg/ml,其次为Ⅳ3,5,7,8和Ⅵ1,2.IC(50)在0.43~0.94mg/ml。化合物Ⅰ,Ⅱ,Ⅳ2,4,6和9虽有抑制作用,但无实际意义。结论:益母草碱具有明显的抗血小板聚集活性,完整的益母草碱分子是维持这种活性的基本结构,改变分子结构碱性胍基为氨基,引入双键或碳链加长以及丁香酸氨基醇酯乙烯化或乙氧羰基化,其活性均比母体化合物强。
OBJECTIVE: To observe and compare the anti-platelet aggregation activity of leucovorin, syringylsterol and syringate aminoalcohol ester compounds and their relationship with structure. METHODS: Platelet aggregation was used as an indicator and IC(50) was calculated to compare the effect of each sample. RESULTS: Leonuridine (I), Compounds II, III and IV1, 2 were able to inhibit the platelet aggregation induced by ADP in rats and rabbits, and the IC (50) was 0.97, 4.4, 5.2, 0 respectively. .36 and 1.14 mg/ml. All compounds inhibited ADP-induced platelet aggregation in rats and rabbits in vitro. The effects of IV1, V1 and VII1, 2 were the strongest, IC (50) was 0.15-0.36 mg/ml, followed by IV3. ,5,7,8 and VI1,2. IC(50) is in the range of 0.43 to 0.94 mg/ml. Although Compounds I, II, IV2, 4, 6 and 9 have inhibitory effects, they have no practical significance. Conclusion: Leonuridine has obvious anti-platelet aggregation activity. The intact leukotriene molecule is the basic structure that maintains this activity. It changes the molecular structure. The basic sulfhydryl group is an amino group, and the introduction of double bond or carbon chain extension and syringate amino alcohol ester ethylene Or ethoxycarbonylation, its activity is stronger than the parent compound.