Tuning Push-Pull Electronic Effects of AIEgens to Boost Theranostic Efficacy for Colon Cancer,Journal of the American Chemical Society

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Tuning Push-Pull Electronic Effects of AIEgens to Boost Theranostic Efficacy for Colon Cancer
Journal of the American Chemical Society ( IF 14.4 ) Pub Date : 2020-06-01 , DOI: 10.1021/jacs.0c02434
Hai-Tao Feng _{1,

2} , Shaomin Zou , Ming Chen ₂ , Feng Xiong ₃ , Mong-Hong Lee , Lekun Fang , Ben Zhong Tang _{2,

4}

Affiliation

Colon cancer is one of the most common cancers with high mortality in humans. Early diagnosis and treatment of colon cancer is of great significance for cancer therapy. Up until now, numerous theranostic agents have been developed to detect and kill cancer cells. However, few reports have focused on how these agents control and affect gene expression of cancer cells in vivo. Herein, three pyridinium-functionalized tetraphenylethylene derivatives (namely TPE-OM, TPE-H and TPE-NO2) with electron-donating and electron-withdrawing groups were facilely synthesized as theranostic agents for cell imaging and anti-colon cancer therapy. Among these AIE luminogens (AIEgens), TPE-OM with donor and acceptor structure showed the best treatment efficacy for colon cancer through systematic biological evaluation and comparison. Both in vitro cell imaging and in vivo tumor treatment experiments demonstrated that TPE-OM can be utilized as an efficient theranostic agent to diagnose and kill colon cancer cells. Flow cytometric analysis revealed that cell cycle process was disturbed by TPE-OM in colon cancer cells. Deep insight into the gene level revealed that the expressions of cell cycle-promoting genes were inhibited upon addition of TPE-OM. This study may open a new venue for unraveling the mechanisms of cancer metastasis.

中文翻译：

调整 AIEgens 的推挽电子效应以提高结肠癌的治疗效果

结肠癌是人类最常见的癌症之一，死亡率很高。结肠癌的早期诊断和治疗对于癌症治疗具有重要意义。到目前为止，已经开发了许多治疗诊断试剂来检测和杀死癌细胞。然而，很少有报道关注这些药物如何控制和影响体内癌细胞的基因表达。在此，我们轻松合成了三种具有给电子和吸电子基团的吡啶鎓功能化四苯基乙烯衍生物（即 TPE-OM、TPE-H 和 TPE-NO2）作为细胞成像和抗结肠癌治疗的治疗诊断剂。在这些AIE发光剂（AIEgens）中，通过系统的生物学评估和比较，具有供体和受体结构的TPE-OM对结肠癌的治疗效果最好。体外细胞成像和体内肿瘤治疗实验均表明，TPE-OM 可作为一种有效的治疗诊断剂来诊断和杀死结肠癌细胞。流式细胞术分析显示，结肠癌细胞中的细胞周期过程受到 TPE-OM 的干扰。对基因水平的深入了解表明，添加 TPE-OM 后，细胞周期促进基因的表达受到抑制。这项研究可能为揭示癌症转移的机制开辟一个新的途径。对基因水平的深入了解表明，添加 TPE-OM 后，细胞周期促进基因的表达受到抑制。这项研究可能为揭示癌症转移的机制开辟一个新的途径。对基因水平的深入了解表明，添加 TPE-OM 后，细胞周期促进基因的表达受到抑制。这项研究可能为揭示癌症转移的机制开辟一个新的途径。

更新日期：2020-06-01

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