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来自桑树的具有蛋白酪氨酸磷酸酶1B抑制活性的异戊烯基化酚类化合物。

Isoprenylated phenolic compounds with PTP1B inhibition from Morus alba.

作者信息

Huang Qing-Hua, Lei Chun, Wang Pei-Pei, Li Jing-Ya, Li Jia, Hou Ai-Jun

机构信息

Department of Pharmacognosy, School of Pharmacy, Fudan University, Shanghai 201203, PR China.

National Center for Drug Screening, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, PR China.

出版信息

Fitoterapia. 2017 Oct;122:138-143. doi: 10.1016/j.fitote.2017.09.006. Epub 2017 Sep 12.

Abstract

Two new Diels-Alder adducts, albasins A and B (1 and 2), one new isoprenylated 2-arylbenzofuran, albasin C (3), one new isoprenylated flavone, albasin D (4), together with sixteen known phenolic compounds, were isolated from the root bark of Morus alba. Their structures were elucidated by extensive spectroscopic analysis, including NMR, MS, and ECD data. All the new compounds and most of the known ones showed significant inhibitory effects on PTP1B in vitro with IC values ranging from 0.57 to 7.49μM.

摘要

从桑白皮中分离得到两个新的狄尔斯-阿尔德加合物,即白桑素A和B(1和2),一个新的异戊烯基化2-芳基苯并呋喃,白桑素C(3),一个新的异戊烯基化黄酮,白桑素D(4),以及十六个已知的酚类化合物。通过广泛的光谱分析,包括核磁共振、质谱和电子圆二色光谱数据,阐明了它们的结构。所有新化合物和大多数已知化合物在体外对蛋白酪氨酸磷酸酶1B(PTP1B)均表现出显著的抑制作用,其半数抑制浓度(IC)值在0.57至7.49μM之间。

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