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来自柔毛水杨梅中华变种的脂肪酸合酶抑制剂。

Fatty acid synthase inhibitors from Geum japonicum Thunb. var. chinense.

作者信息

Liu Hongwei, Li Jiankuan, Zhao Wenhua, Bao Li, Song Xiaohong, Xia Ying, Wang Xue, Zhang Chao, Wang Xiaozhu, Yao Xinsheng, Li Ming

机构信息

Institute of Microbiology, Chinese Academy of Sciences, No. 8 Zhongguancun Beiertiao Road, Haidian District, Beijing, P. R. China.

出版信息

Chem Biodivers. 2009 Mar;6(3):402-10. doi: 10.1002/cbdv.200700462.

Abstract

Bioassay-guided fractionation of the MeOH extract of Geum japonicum Thunb. var. chinense using the fatty acid synthase inhibition assay led to the isolation of a new dimeric ellagitannin, gemin G (1), together with six known compounds, gemin A (2), casuarinin (3), pedunculagin (4), potentillin (5) , tellimagrandin II (6), and ellagic acid (7). Their structures were determined on the basis of spectroscopic analyses. Compounds 1-7 displayed strong inhibitory activities on fatty acid synthase with IC(50) values in the range of 0.21-41.4 microM. Compounds 1-4 exhibited significant antioxidant activities higher than vitamin C in the ORAC assay. Compounds 1 and 2 also showed weak cytotoxic effects on BGC-823 cell.

摘要

采用脂肪酸合酶抑制试验对柔毛水杨梅变种中华水杨梅的甲醇提取物进行生物活性导向的分离,得到了一种新的二聚体鞣花单宁,即双聚体G(1),以及六种已知化合物,双聚体A(2)、杨梅亭(3)、地锦素(4)、 potentillin(5)、tellimagrandin II(6)和鞣花酸(7)。通过光谱分析确定了它们的结构。化合物1-7对脂肪酸合酶显示出较强的抑制活性,IC50值在0.21-41.4微摩尔范围内。在氧自由基吸收能力(ORAC)试验中,化合物1-4表现出显著高于维生素C的抗氧化活性。化合物1和2对BGC-823细胞也显示出较弱的细胞毒性作用。

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