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体外白藜芦醇寡聚物对芍药种子提取物中 BACE-1 的抑制活性。

In vitro BACE-1 inhibitory activity of resveratrol oligomers from the seed extract of Paeonia lactiflora.

机构信息

Korea Research Institute of Chemical Technology, Daejeon, Korea.

出版信息

Planta Med. 2011 Mar;77(4):374-6. doi: 10.1055/s-0030-1250370. Epub 2010 Oct 1.

Abstract

A new resveratrol oligomer (1) together with eight related components (2- 9) were isolated from the seed extract of Paeonia lactiflora (Paeoniaceae) as active principles responsible for the inhibition of beta-site APP-cleaving enzyme 1 (BACE-1) in vitro. The chemical structure of 1 was established as (-)-7a,8a- CIS- ε-viniferin with the aid of spectroscopic analyses including NOESY experiments. All isolated resveratrol oligomers (1- 9) demonstrated significant inhibition on baculovirus-expressed BACE-1 in a dose-dependent manner, which was assessed by the FRET assay using Rh-EVNLDAEFK as a substrate in vitro.

摘要

从牡丹(毛茛科)种子提取物中分离得到一种新的白藜芦醇低聚物(1)和 8 种相关成分(2-9),这些物质是体外抑制β-位点 APP 裂解酶 1(BACE-1)的活性成分。1 的化学结构被确定为(-)-7a,8a-CIS-ε-viniferin,这得益于包括 NOESY 实验在内的光谱分析。所有分离得到的白藜芦醇低聚物(1-9)在体外通过使用 Rh-EVNLDAEFK 作为底物的 FRET 测定,均表现出对杆状病毒表达的 BACE-1 的显著抑制作用,且这种抑制作用呈剂量依赖性。

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