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首页> 外文期刊>Advanced Functional Materials >Tumor Inhibition Achieved by Targeting and Regulating Multiple Key Elements in EGFR Signaling Pathway Using a Self-Assembled Nanoprodrug
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Tumor Inhibition Achieved by Targeting and Regulating Multiple Key Elements in EGFR Signaling Pathway Using a Self-Assembled Nanoprodrug

机译：通过使用自组装的纳米前体药物靶向和调节EGFR信号通路中的多个关键元素来实现肿瘤抑制

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摘要

Comprehensive understanding of signaling pathways regulating cancer progression has led to tremendous advances of molecularly targeted therapies. The epidermal growth factor receptor (EGFR) pathway is an attractive target for cancer therapy, and targeting multiple key elements in the pathway may further facilitate therapeutic efficacy. Here, an EGFR-targeted nanoprodrug is demonstrated for in vivo imaging and tumor inhibition, which is assembled by a disulfide-bridged quercetin (QSSQ) and an EGFR inhibitor erlotinib. QSSQ is synthesized via chemical manipulation of multiple phenolic hydroxyl groups on quercetin; and the nanoprodrug is then fabricated through the disulfide-facilitated assembly of QSSQ and erlotinib. The nanoprodrug is of high drug loading (87.3%) since its only inert component is the disulfide linker. The nanoprodrug is stable in physiological environment, whereas overexpressed glutathione in tumor tissue breaks the disulfide bridge, thereby disrupting the nanostructure and releasing active drugs quercetin and erlotinib. Upon release, erlotinib serves as an active drug blocking the EGFR tyrosine kinase, and quercetin generates strong aggregation-induced emission of fluorescence for imaging drug release and acts as another drug inhibiting the downstream EFGR signaling, as evidenced by Western blotting analyses. The combined action thereof results in remarkable antitumor efficacy toward xenograft tumor-bearing mice.
机译：对调节癌症进程的信号通路的全面理解已导致分子靶向疗法的巨大进步。表皮生长因子受体（EGFR）途径是癌症治疗的诱人靶标，靶向该途径中的多个关键元素可能会进一步促进治疗功效。在这里，证明了靶向EGFR的纳米前药可用于体内成像和肿瘤抑制，它是由二硫键连接的槲皮素（QSSQ）和EGFR抑制剂厄洛替尼组装而成的。 QSSQ是通过槲皮素上多个酚羟基的化学操作合成的；然后通过QSSQ和厄洛替尼的二硫化物促进组装来制备纳米前药。纳米前药具有很高的载药量（87.3％），因为它的唯一惰性成分是二硫键。纳米前药在生理环境中稳定，而肿瘤组织中过表达的谷胱甘肽破坏了二硫键，从而破坏了纳米结构并释放了槲皮素和厄洛替尼活性药物。释放后，厄洛替尼用作阻断EGFR酪氨酸激酶的活性药物，槲皮素产生强烈的聚集诱导的荧光发射，用于成像药物释放，并充当另一种抑制下游EFGR信号传导的药物，如Western印迹分析所证明。它们的联合作用导致了对异种移植荷瘤小鼠的显着抗肿瘤功效。

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  • 来源
    《Advanced Functional Materials》 |2018年第22期|1800692.1-1800692.15|共15页
  • 作者

    Li Bowen; Xie Xin; Chen Zelin; Zhan Chenyue; Zeng Fang; Wu Shuizhu;

  • 作者单位

    South China Univ Technol, Coll Mat Sci & Engn, State Key Lab Luminescent Mat & Devices, Wushan Rd 381, Guangzhou 510640, Guangdong, Peoples R China;

    South China Univ Technol, Coll Mat Sci & Engn, State Key Lab Luminescent Mat & Devices, Wushan Rd 381, Guangzhou 510640, Guangdong, Peoples R China;

    South China Univ Technol, Coll Mat Sci & Engn, State Key Lab Luminescent Mat & Devices, Wushan Rd 381, Guangzhou 510640, Guangdong, Peoples R China;

    South China Univ Technol, Coll Mat Sci & Engn, State Key Lab Luminescent Mat & Devices, Wushan Rd 381, Guangzhou 510640, Guangdong, Peoples R China;

    South China Univ Technol, Coll Mat Sci & Engn, State Key Lab Luminescent Mat & Devices, Wushan Rd 381, Guangzhou 510640, Guangdong, Peoples R China;

    South China Univ Technol, Coll Mat Sci & Engn, State Key Lab Luminescent Mat & Devices, Wushan Rd 381, Guangzhou 510640, Guangdong, Peoples R China;

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  • 正文语种 eng
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  • 关键词

    EGFR pathway; erlotinib; nanoprodrugs; quercetin; tumor imaging; tumor inhibition;

    机译：EGFR通路;厄洛替尼;纳米药物;槲皮素;肿瘤显像;肿瘤抑制;

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