作者:Chun-Nan Lin、Hsin-Kaw Hsieh、Shiou-Jyh Liou、Horng-Huey Ko、Hsien-Cheng Lin、Mei-Ing Chung、Feng-Nien Ko、Hong-Wen Liu、Che-Ming Teng
DOI:10.1111/j.2042-7158.1996.tb05994.x
日期:2011.4.12
A series of xanthone derivatives was synthesized and tested in-vitro for their ability to inhibit aggregation of rabbit washed platelets and human platelet-rich plasma (PRP) induced by various inducers. 2-Prenyloxyxanthone showed the most potent inhibition of rabbit washed platelet aggregation induced by arachidonic acid (1C50 = 10.2 microM). Of the compounds tested in human PRP, 2-[3 (propylamino
合成了一系列的an吨酮衍生物,并体外测试了它们抑制各种诱导物诱导的兔洗出的血小板和富含人血小板的血浆(PRP)聚集的能力。2-Penyloxyxanthone对花生四烯酸(1C50 = 10.2 microM)诱导的兔洗净血小板凝集的抑制作用最强。在人PRP中测试的化合物中,2- [3(丙基氨基)-2-羟基丙氧基]蒽酮(4)盐酸盐表现出对肾上腺素诱导的血小板聚集的最强抑制作用(IC50 = 4.4 microM),而在小鼠抗血栓形成评估中活性,化合物4表现出最有效的保护小鼠免受血栓形成的攻击。化合物4、2- [3-(异丙基氨基)-2-羟基丙氧基l吨酮盐酸盐和 5二羟基黄酮抑制人肾上腺素诱导的肾上腺素的次级聚集。我们得出结论,这些化合物的抗血小板作用主要是由于对血栓烷形成的抑制作用。