Tuning Push-Pull Electronic Effects of AIEgens to Boost the Theranostic Efficacy for Colon Cancer
Tuning Push-Pull Electronic Effects of AIEgens to Boost the Theranostic Efficacy for Colon Cancer
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调节 AIEgens 的推挽电子效应以提高结肠癌的治疗效率
DOI：
10.1021/jacs.0c02434
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发表时间：
2020-07-01
影响因子：
15
通讯作者：
Tang, Ben Zhong
中科院分区：
文献类型：
--
作者：
Feng, Hai-Tao;Zou, Shaomin;Tang, Ben Zhong
结肠癌是人类死亡率高的最常见癌症之一。结肠癌的早期诊断和治疗对癌症治疗具有重要意义。已经开发了许多疗法剂来检测和杀死癌细胞。但是，很少有报道集中在这些药物如何控制和影响体内癌细胞的基因表达。在此，三个吡啶官官能化的四苯基乙烯衍生物，即TPE-OK TPE-H和TPE-NO2，具有电子含电子和吸电子基团，作为细胞成像和抗果仁癌治疗的治疗剂。在这些AIE发光剂（AIEGEN）中，具有供体结构的TPE-OM通过系统的生物学评估和比较显示出对结肠癌的最佳治疗功效。体外细胞成像和体内肿瘤治疗实验均表明，TPE-OM可以用作有效的疗法剂来诊断和杀死结肠癌细胞。流式细胞仪分析表明，结肠癌细胞中TPE-OM干扰了细胞周期过程。对基因水平的深入了解表明，添加TPE-OM后抑制了细胞周期促进基因的表达。这项研究可能会为揭开癌症转移机制的新场地。
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. Numerous theranostic agents have been developed to detect and kill cancer cells. However, few reports have focused on how these agents control and affect the gene expression of cancer cells in vivo. Herein, three pyridinium-functionalized tetraphenylethylene derivatives, namely, TPE-OK TPE-H, and TPE-NO2, with electron-donating and electron-withdrawing groups were facilely synthesized as theranostic agents for cell imaging and anticolon 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 the 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 was inhibited upon addition of TPE-OM. This study may open a new venue for unraveling the mechanisms of cancer metastasis.