Yu Yang, Gan Li-She, Yang Sheng-Ping, Sheng Li, Liu Qun-Fang, Chen Shao-Nong, Li Jia, Yue Jian-Min
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences , Shanghai 201203, People's Republic of China.
Institute of Modern Chinese Medicine, College of Pharmaceutical Sciences, Zhejiang University , Hangzhou 310058, People's Republic of China.
J Nat Prod. 2016 May 27;79(5):1365-72. doi: 10.1021/acs.jnatprod.6b00090. Epub 2016 May 4.
Nine new conjugates of sesquiterpenoids and acylphloroglucinols, named eucarobustols A-I (1-9), as well as 11 known analogues were isolated from the leaves of Eucalyptus robusta. The sesquiterpenoid motifs furnishing the new conjugates included four structural types of aristolane (1 and 2), guaiane (3), eudesmane (4), and aromadendrane (5-9) moieties. Compounds 1 and 2 were found to represent the first examples of conjugates of aristolane and acylphloroglucinol units. In turn, compound 3 features a new coupling model of guaiane and acylphloroglucinol via the C-4-C-7' bond. Compounds 1, 7, and 9 showed inhibitory activities against protein tyrosine phosphatase 1B (PTP1B) with IC50 values of 1.3, 1.8, and 1.6 μM, respectively.
从大叶桉树叶中分离出9种新的倍半萜类与酰基间苯三酚的共轭物，命名为尤卡罗布醇A - I（1 - 9），以及11种已知类似物。构成新共轭物的倍半萜基序包括四种结构类型的马兜铃烷（1和2）、愈创木烷（3）、桉叶烷（4）和香树烷（5 - 9）部分。化合物1和2是马兜铃烷与酰基间苯三酚单元共轭物的首个实例。相应地，化合物3具有通过C - 4 - C - 7'键连接的愈创木烷和酰基间苯三酚的新偶联模式。化合物1、7和9对蛋白酪氨酸磷酸酶1B（PTP1B）具有抑制活性，IC50值分别为1.3、1.8和1.6 μM。
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