Applová Lenka, Karlíčková Jana, Říha Michal, Filipský Tomáš, Macáková Kateřina, Spilková Jiřina, Mladěnka Přemysl
Department of Pharmacology and Toxicology, Faculty of Pharmacy in Hradec Králové, Charles University, Akademika Heyrovského 1203, 500 05 Hradec Králové, Czech Republic.
Department of Pharmaceutical Botany and Ecology, Faculty of Pharmacy in Hradec Králové, Charles University, Akademika Heyrovského 1203, 500 05 Hradec Králové, Czech Republic.
Phytomedicine. 2017 Nov 15;35:11-17. doi: 10.1016/j.phymed.2017.08.023. Epub 2017 Aug 24.
One reason for the lower incidence of cardiovascular diseases in Asian countries may be the high intake of isoflavonoids and their antiplatelet effects may be an important factor. To date, there is limited comparison of a range of isoflavonoids and knowledge of their effects at different levels of platelet aggregation.
To screen the antiplatelet effects of a number of isoflavonoids on the arachidonic acid based aggregation pathway and investigate how the antiplatelet activity might occur.
The antiplatelet effects were first screened in whole human blood where platelet aggregation was induced by arachidonic acid. Further analysis was targeted at search of the mechanism of action.
Thirteen of the eighteen tested isoflavonoids had significant inhibitory effect on platelet aggregation in whole human blood. Genistein had the same potency as clinically used acetylsalicylic acid (ASA) while tectorigenin was clearly stronger than ASA. Further analyses showed that the effect of tectorigenin was not based on inhibition of cyclooxygenase-1 in contrast to ASA or thromboxane synthase but by competitive antagonism at thromboxane receptors.
Tectorigenin is a more potent antiplatelet compound than ASA and thus an interesting substance for further testing.
亚洲国家心血管疾病发病率较低的一个原因可能是异黄酮的高摄入量，其抗血小板作用可能是一个重要因素。迄今为止，对一系列异黄酮的比较有限，且对其在不同血小板聚集水平下的作用了解不足。
筛选多种异黄酮对基于花生四烯酸的聚集途径的抗血小板作用，并研究抗血小板活性可能如何发生。
首先在全血中筛选抗血小板作用，其中血小板聚集由花生四烯酸诱导。进一步分析旨在寻找作用机制。
18种受试异黄酮中的13种对全血中的血小板聚集有显著抑制作用。染料木黄酮的效力与临床使用的乙酰水杨酸（ASA）相同，而鸢尾黄酮明显强于ASA。进一步分析表明，与ASA或血栓素合酶不同，鸢尾黄酮的作用并非基于对环氧合酶-1的抑制，而是通过对血栓素受体的竞争性拮抗作用。
鸢尾黄酮是一种比ASA更有效的抗血小板化合物，因此是一种值得进一步测试的有趣物质。
