Natural product-based design, synthesis and biological evaluation of Albiziabioside A derivatives that selectively induce HCT116 cell death
Natural product-based design, synthesis and biological evaluation of Albiziabioside A derivatives that selectively induce HCT116 cell death
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基于天然产物的选择性诱导HCT116细胞死亡的合欢双苷A衍生物的设计、合成和生物学评价
DOI：
10.1016/j.ejmech.2015.12.034
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发表时间：
2016
影响因子：
6.7
通讯作者：
Maosheng Cheng
中科院分区：
文献类型：
--
作者：
Gaofei Wei;Shanshan Cui;Weijing Luan;Shuai Wang;Zhuang Hou;Yongxiang Liu;Yang Liu;Maosheng Cheng
设计并合成了一系列肉桂酰衍生物的合欢双苷A偶联取代基。使用 MTT 测定筛选合成的化合物针对六种人类癌细胞系的抗癌活性。合成衍生物显示出优异的选择性，因为它们仅对 HCT116 细胞系有毒。与阳性对照相比，一些化合物对 HCT116 表现出更好的抗癌活性，例如 5-氟尿嘧啶和合欢苷 A。Compound8n 是最活跃的衍生物。重要的是，还发现8n的抗增殖活性可能归因于诱导HCT116细胞的细胞周期停滞和细胞凋亡。
A series of Albiziabioside A coupled substituents of cinnamoyl derivatives were designed and synthesized. The synthesized compounds were screened for anticancer activity against a panel of six human cancer cell lines using a MTT assay. Synthetic derivatives showed excellent selectivity, as they were toxic against only HCT116 cell line. Some compounds exhibited better anti-cancer activity against HCT116 compared to positive controls, such as 5-fluorouracil and Albiziabioside A. Compound8nwas the most active derivative. Importantly, it was also found that the anti-proliferative activity of8ncould be attributed to the induction of cell cycle arrest and apoptosis in HCT116 cells.