Programa de Pós-Graduação em Química, Universidade Federal de Santa Catarina, Florianópolis, SC, Brazil.
Bioorg Med Chem. 2012 May 1;20(9):3016-30. doi: 10.1016/j.bmc.2012.03.001. Epub 2012 Mar 15.
Two cucurbitacins, dihydrocucurbitacin B (1) and cucurbitacin B (2), which can be obtained in large amounts from the roots of Wilbrandia ebracteata and from the fruits of Luffa operculata, respectively, were used as starting materials for the preparation of a library of 29 semi-synthetic derivatives. The structural changes that were performed include the removal, modification or permutation of functional groups in rings A and B as well as in the side chain. All new semisynthetic compounds, as well as 1 and 2, were tested in vitro for their cytotoxic effects on non-small-cell lung cancer cells (A549 cells). Some of these compound displayed potent to moderate activity against A549 tumor cells, especially those cucurbitacin B derivatives which were modified at ring A.
两种葫芦素，分别是二氢葫芦素 B（1）和葫芦素 B（2），可以从卫矛的根和丝瓜的果实中大量获得，分别作为制备 29 个半合成衍生物文库的起始材料。进行的结构变化包括去除、修饰或改变 A 环和 B 环以及侧链中的功能基团。所有新的半合成化合物以及 1 和 2 都在体外测试了对非小细胞肺癌细胞（A549 细胞）的细胞毒性作用。其中一些化合物对 A549 肿瘤细胞表现出较强到中等的活性，特别是那些在 A 环上修饰的葫芦素 B 衍生物。
