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来自中国海洋海绵龟甲肉芝软珊瑚的具有蛋白酪氨酸磷酸酶-1B抑制活性的溴化多不饱和脂质。

Brominated polyunsaturated lipids with protein tyrosine phosphatase-1B inhibitory activity from Chinese marine sponge Xestospongia testudinaria.

作者信息

He Wen-Fei, Liang Lin-Fu, Cai You-Sheng, Gao Li-Xin, Li Yu-Fen, Li Jia, Liu Hai-Li, Guo Yue-Wei

机构信息

a School of Pharmaceutical Sciences, Wenzhou Medical University , Wenzhou 325035 , China.

出版信息

J Asian Nat Prod Res. 2015;17(8):861-6. doi: 10.1080/10286020.2015.1026334. Epub 2015 Apr 1.

Abstract

A new brominated polyunsaturated lipid, methyl (E,E)-14,14-dibromo-4,6,13-tetradecatrienoate (1), along with three known related analogues (2-4), were isolated from the Et2O-soluble portion of the acetone extract of Chinese marine sponge Xestospongia testudinaria treated with diazomethane. The structure of the new compound was elucidated by detailed spectroscopic analysis and by comparison with literature data. Compound 3 exhibited significant inhibitory activity against protein tyrosine phosphatase 1B (PTP1B), a key target for the treatment of type II diabetes and obesity, with an IC50 value of 5.30 ± 0.61 μM, when compared to the positive control oleanolic acid (IC50 = 2.39 ± 0.26 μM).

摘要

从用重氮甲烷处理过的中国海洋海绵龟甲海绵(Xestospongia testudinaria)丙酮提取物的二氯甲烷可溶部分中,分离出一种新的溴化多不饱和脂质,即甲基(E,E)-14,14-二溴-4,6,13-十四碳三烯酸酯(1),以及三种已知的相关类似物(2-4)。通过详细的光谱分析并与文献数据比较,阐明了新化合物的结构。与阳性对照齐墩果酸(IC50 = 2.39 ± 0.26 μM)相比,化合物3对蛋白酪氨酸磷酸酶1B(PTP1B)表现出显著的抑制活性,PTP1B是治疗II型糖尿病和肥胖症的关键靶点,其IC50值为5.30 ± 0.61 μM。

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