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从桉树中提取的强效 HGF/c-Met 轴抑制剂：苯丙三醇和倍半萜的偶联对活性至关重要。

Potent HGF/c-Met axis inhibitors from Eucalyptus globulus: the coupling of phloroglucinol and sesquiterpenoid is essential for the activity.

机构信息

State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Zhangjiang Hi-Tech Park, Shanghai, 201203, People's Republic of China.

出版信息

J Med Chem. 2012 Sep 27;55(18):8183-7. doi: 10.1021/jm3007454. Epub 2012 Sep 7.

DOI:10.1021/jm3007454
PMID:22934600
Abstract

Eucalyptin A (1), together with two known compounds 2 and 3 exhibiting potent inhibition on HGF/c-Met axis, was discovered from the fruits of Eucalyptus globulus. 1 possessed an unprecedented carbon framework of phloroglucinol-coupled sesquiterpenoid, and its structure was elucidated by spectroscopic method and ECD calculation. A brief structure-activity relationship discussion indicated that the coupling of a phloroglucinol and a sesquiterpenoid is essential for the activity.

摘要

从桉树果实中发现了桉树素 A（1），以及另外两种具有强烈抑制 HGF/c-Met 轴作用的已知化合物 2 和 3。1 具有前所未有的苯丙三醇偶联倍半萜碳骨架，其结构通过光谱方法和 ECD 计算阐明。简要的构效关系讨论表明，苯丙三醇和倍半萜的偶联对于活性是必不可少的。

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