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Platelet-Activating Factor (PAF) Antagonistic Activity of a New Biflavonoid from Garcinia nervosa var. pubescens King

机译:一种新的藤黄双黄酮的血小板活化因子(PAF)拮抗活性。耻骨王

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摘要

The methanol extract of the leaves of Garcinia nervosa var. pubescens King, which showed strong inhibitory effects on platelet-activating factor (PAF) receptor binding, was subjected to bioassay-guided isolation to obtain a new biflavonoid, II-3,I-5, II-5,II-7,I-4',II-4'-hexahydroxy-(I-3,II-8)-flavonylflavanonol together with two known flavonoids, 6-methyl-4'-methoxyflavone and acacetin. The structures of the compounds were elucidated by spectroscopic methods. The compounds were evaluated for their ability to inhibit PAF receptor binding to rabbit platelets using 3H-PAF as a ligand. The biflavonoid and acacetin showed strong inhibition with IC50 values of 28.0 and 20.4 µM, respectively. The results suggest that these compounds could be responsible for the strong PAF antagonistic activity of the plant.
机译:藤黄叶的甲醇提取物。对人体的血小板活化因子(PAF)受体结合具有强烈抑制作用的pubescens King经过生物测定指导的分离,获得了新的双黄酮类化合物II-3,I-5,II-5,II-7,I- 4',II-4'-六羟基-(I-3,II-8)-黄酮基黄烷醇与两种已知的类黄酮,6-甲基-4'-甲氧基黄酮和醋氨蝶呤。通过光谱方法阐明了化合物的结构。使用 3 H-PAF作为配体评估了这些化合物抑制PAF受体与兔血小板结合的能力。双黄酮类和醋氨蝶呤显示出强烈的抑制作用,IC50值分别为28.0和20.4 µM。结果表明这些化合物可能是植物强大的PAF拮抗活性的原因。

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