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白芷的苯并呋喃和香豆素衍生物及其对 PPAR-γ 的配体结合活性。

Benzofuran and coumarin derivatives from the root of Angelica dahurica and their PPAR-γ ligand-binding activity.

机构信息

Tokyo University of Pharmacy and Life Sciences, School of Pharmacy, 1432-1 Horinouchi, Hachioji, Tokyo, 192-0392, Japan.

Tokyo University of Pharmacy and Life Sciences, School of Pharmacy, 1432-1 Horinouchi, Hachioji, Tokyo, 192-0392, Japan.

出版信息

Phytochemistry. 2020 May;173:112301. doi: 10.1016/j.phytochem.2020.112301. Epub 2020 Feb 21.

DOI:10.1016/j.phytochem.2020.112301
PMID:32092557
Abstract

A phytochemical investigation of the root of Angelica dahurica led to the isolation of benzofuran and coumarin derivatives. This is the first report of the isolation and identification of three furanocoumarin sulfates from A. dahurica root. The structures of a total of twelve undescribed compounds were determined by extensive spectroscopic analysis, including 2D NMR data, hydrolysis, and solvolysis, followed by either physicochemical and spectroscopic data or X-ray crystallographic analysis. The isolated compounds were evaluated for their PPAR-γ ligand-binding activity, and six compounds showed significant PPAR-γ ligand-binding activity. In particular, the undescribed benzofuran derivative, 3-[6,7-furano-9-hydroxy-4-(2″,3″-dihydroxy-3″-methylbutyloxy)]-phenyl propionic acid, exhibited the most potent PPAR-γ ligand-binding activity and accumulated intracellular lipid in 3T3-L1 cells.

摘要

对白芷根的植物化学研究导致了苯并呋喃和香豆素衍生物的分离。这是首次从白芷根中分离和鉴定三种呋喃香豆素硫酸盐。通过广泛的光谱分析,包括 2D NMR 数据、水解和溶剂解,以及物理化学和光谱数据或 X 射线晶体学分析,确定了总共 12 种未描述化合物的结构。对分离得到的化合物进行了 PPAR-γ 配体结合活性评价,其中 6 种化合物表现出显著的 PPAR-γ 配体结合活性。特别是,未描述的苯并呋喃衍生物 3-[6,7-呋喃-9-羟基-4-(2″,3″-二羟基-3″-甲基丁氧基)]-苯丙酸,表现出最强的 PPAR-γ 配体结合活性,并在 3T3-L1 细胞中积累细胞内脂质。

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Phytochemistry. 2020 May;173:112301. doi: 10.1016/j.phytochem.2020.112301. Epub 2020 Feb 21.
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