Synthesis and in vitro anticancer activities of novel aryl-naphthalene lignans

Jie Hui; Yu Zhao; Li Zhu

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Synthesis and in vitro anticancer activities of novel aryl-naphthalene lignans

机译：新型芳基萘木脂素的合成及体外抗癌活性

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Cancer is one of the leading causes of death in the world. In this study, a series of novel aryl-naphthalene lignans were synthesized and the inhibitory effects of all compounds on cancer cells growth were investigated. The target compounds were structurally characterized by 1H NMR, 13C NMR, IR and HRMS. The IC50 of these compounds on three tumor cell lines A549, SW480, KB and one normal cell line HEK293 were obtained by MTT assay. Compound 6′i, which has a para-methyl on the D-ring indicated potent anti-tumor activities and the IC50 of this compound on KB cells was 18.9 μM. But this compound showed low cytotoxicity on normal cell line HEK293. Furthermore, fluorescent double staining indicated that compound 6′i induced apoptosis of KB cells. Western blot analysis showed Compound 6′i increased the expression of cleaved-caspase-3 and bax, reduced the expression of bcl-2.

机译：癌症是世界上主要的死亡原因之一。在这项研究中，合成了一系列新型的芳基萘木脂素，并研究了所有化合物对癌细胞生长的抑制作用。通过1 H NMR，13 C NMR，IR和HRMS对目标化合物进行结构表征。通过MTT法获得了这些化合物在三种肿瘤细胞系A549，SW480，KB和一种正常细胞系HEK293上的IC50 。在D环上具有对甲基的化合物6'i具有较强的抗肿瘤活性，该化合物对KB细胞的IC50 为18.9μM。但是这种化合物对正常细胞系HEK293的细胞毒性较低。此外，荧光双重染色表明化合物6'i诱导了KB细胞的凋亡。 Western印迹分析表明，化合物6'i增加了裂解的caspase-3和bax的表达，降低了bcl-2的表达。

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来源
《Medicinal Chemistry Research》 |2012年第12期|p.3994-4001|共8页
作者
Jie Hui; Yu Zhao; Li Zhu;
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作者单位

Institute of Nautical Medicine, Nantong University, Nantong, 226001, China;

Institute of Nautical Medicine, Nantong University, Nantong, 226001, China;

Institute of Nautical Medicine, Nantong University, Nantong, 226001, China;

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原文格式 PDF
正文语种 eng
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关键词
Diphyllin; Antitumor; Apoptosis; Synthesis;

机译：双叶抑素;抗肿瘤;凋亡;合成;

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Synthesis and in vitro anticancer activities of novel aryl-naphthalene lignans

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