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来自软毛南酸枣 Garcinia nervosa var. pubescens King 的新双黄酮具有血小板激活因子 (PAF)拮抗活性。

Platelet-activating factor (PAF) antagonistic activity of a new biflavonoid from Garcinia nervosa var. pubescens King.

机构信息

Drug and Herbal Research Centre, Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Jalan Raja Muda Abdul Aziz, 50300 Kuala Lumpur, Malaysia.

出版信息

Molecules. 2012 Sep 10;17(9):10893-901. doi: 10.3390/molecules170910893.

Abstract

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.

摘要

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。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ccd5/6268030/f02fef389633/molecules-17-10893-g001.jpg

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