Drug and Herbal Research Centre, Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Jalan Raja Muda Abdul Aziz, 50300 Kuala Lumpur, Malaysia.
Molecules. 2012 Sep 10;17(9):10893-901. doi: 10.3390/molecules170910893.
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.
杨桃科藤山柳属植物显齿蛇葡萄叶甲醇提取物对血小板活化因子(PAF)受体具有较强的抑制作用,采用生物活性跟踪分离方法,从中分离得到一个新的二氢黄酮醇,即 II-3,I-5, II-5,II-7,I-4',II-4'-六羟基(I-3,II-8)-二氢黄酮基二氢黄酮醇,同时还分离得到两个已知的黄酮类化合物,即 6-甲基-4'-甲氧基黄酮和芹菜素。通过波谱方法解析了这些化合物的结构。采用 ³H-PAF 作为配体,评价了这些化合物对兔血小板 PAF 受体结合的抑制能力。该二氢黄酮醇和芹菜素的抑制活性较强,IC₅₀ 值分别为 28.0 和 20.4 μM。结果表明,这些化合物可能是该植物具有较强的 PAF 拮抗活性的原因。