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首页> 外文期刊>Chemical biology and drug design >Design, Synthesis and Biological Evaluation of Cinnamic Acyl Shikonin Derivatives
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Design, Synthesis and Biological Evaluation of Cinnamic Acyl Shikonin Derivatives

机译：肉桂酸紫草素衍生物的设计，合成及生物评价

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摘要

Inducing apoptosis is an important and promising therapeutic approach to overcome cancer. Here, we described a series of novel synthesized compounds, cinnamic acyl shikonin derivatives (1b-19b), which were synthesized starting from shikonin and cinnamic acids, which exhibit anticancer activity via inducing apoptosis in vitro. Our flow cytometry results showed that compound 8b((E)-1-(5,8-dihydroxy-1,4-dioxo-1, 4-dihydronaphthalen-2-yl)-4-methylpent -3-enyl-3-(3-(trifluoromethyl) phenyl)acrylate) (IC_(50) = 0.69, 0.65, 1.62 μM for human SW872-s, A875 and A549 cell lines, respectively) exhibited conspicuous anticancer activities and has low cell toxicity in vitro. Therefore, we considered that compound 8b is potentially to be a candidate of anticancer agent. The proliferation inhibitory effect of compound 8b was associated with its apoptosis-inducing effect by activating caspase-3, caspase-7, caspase-9, and PARP. When the level of cleaved caspase-3, cleaved caspase-7, cleaved caspase-9, and cleaved PARP are rise, apoptosis of cancer cells will be induced.
机译：诱导细胞凋亡是克服癌症的重要且有希望的治疗方法。在这里，我们描述了一系列新合成的化合物，肉桂酸紫草素紫草素衍生物（1b-19b），它们是从紫草素和肉桂酸开始合成的，它们通过诱导体外细胞凋亡表现出抗癌活性。我们的流式细胞仪结果表明化合物8b（（E）-1-（5,8-dihydroxy-1,4-dioxo-1，4-dihydronaphthalen-2-yl）-4-methylpent -3-enyl-3-（ 3-（三氟甲基）苯基）丙烯酸酯）（对于人SW872-s，A875和A549细胞系，IC_（50）= 0.69、0.65、1.62μM）具有显着的抗癌活性，并且在体外具有较低的细胞毒性。因此，我们认为化合物8b可能是抗癌药的候选物。通过激活caspase-3，caspase-7，caspase-9和PARP，化合物8b的增殖抑制作用与其诱导凋亡的作用有关。当裂解的caspase-3，裂解的caspase-7，裂解的caspase-9和裂解的PARP的水平升高时，将诱导癌细胞的凋亡。

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