Cantharidin derivatives from the medicinal insect Mylabris phalerata
Cantharidin derivatives from the medicinal insect Mylabris phalerata
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来自药用昆虫斑蝥 (Mylabris phalerata) 的斑蝥素衍生物
DOI：
10.1016/j.tet.2017.08.034
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发表时间：
2017-10-05
期刊：
影响因子：
2.1
通讯作者：
Ye, Wen-Cai
中科院分区：
文献类型：
--
作者：
Deng, Yuan-Yuan;Zhang, Wei;Ye, Wen-Cai
从斑羚中分离得到13个新的斑腿草素衍生物，包括6个斑泻亚胺-氨基酸加合物(1-6)、5个斑泻亚胺二聚体(7-11)和2个斑泻亚胺-芳香族化合物杂化化合物(12-13)。化合物1-5是第一个通过斑泻亚胺和中性氨基酸结合的天然产物。化合物7-11是第一个由两个不同的斑驳亚胺核组成的斑驳二聚体。通过核磁共振谱、单晶X-射线衍射谱和半合成等手段对其绝对构型进行了表征。化合物6对HepG2、A549和MDA-MB-231细胞有较弱的细胞毒作用，IC50值分别为15.70+/-3.06、20.67+/-4.05和23.79+/-4.54 mU/M。(C)爱思唯尔有限公司发布的2017年。
Thirteen new cantharidin derivatives including six cantharimide-amino acid adducts (1-6), five cantharimide dimers (7-11) and two cantharimide-aromatic compound hybrids (12-13) were isolated from Mylabris phalerata Pallas. Compounds 1-5 represent the first natural products combined through cantharimide and neutral amino acids. Compounds 7-11 are the first cantharimide dimers consisting of two different cantharimide cores. Their structures with absolute configurations were elucidated by means of NMR spectroscopy, single-crystal X-ray diffraction, and semi-synthesis. Compound 6 showed weak cytotoxicity against HepG2, A549 and MDA-MB-231 cells with IC50 values of 15.70 +/- 3.06, 20.67 +/- 4.05 and 23.79 +/- 4.54 mu M, respectively. (C) 2017 Published by Elsevier Ltd.