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Designed DNA nanostructure grafted with erlotinib for non-small-cell lung cancer therapy
Nanoscale ( IF 5.8 ) Pub Date : 2020-11-17 , DOI: 10.1039/d0nr06945k Yuqi Wang 1, 2, 3, 4, 5 , Jin Cheng 2, 4, 5, 6, 7 , Di Zhao 2, 4, 5, 6, 7 , Yan Liu 2, 4, 5, 6, 7 , Tao Luo 2, 4, 5, 6, 7 , Yi-Fang Zhong 2, 4, 5, 6, 7 , Fangli Mo 2, 4, 5, 6, 7 , Xiang-Yang Kong 1, 2, 3, 4 , Jie Song 2, 4, 5, 6, 7
Nanoscale ( IF 5.8 ) Pub Date : 2020-11-17 , DOI: 10.1039/d0nr06945k Yuqi Wang 1, 2, 3, 4, 5 , Jin Cheng 2, 4, 5, 6, 7 , Di Zhao 2, 4, 5, 6, 7 , Yan Liu 2, 4, 5, 6, 7 , Tao Luo 2, 4, 5, 6, 7 , Yi-Fang Zhong 2, 4, 5, 6, 7 , Fangli Mo 2, 4, 5, 6, 7 , Xiang-Yang Kong 1, 2, 3, 4 , Jie Song 2, 4, 5, 6, 7
Affiliation
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Chemotherapy for non-small-cell lung cancer (NSCLC) treatment has been employed over the past 20 years. However, poor water-solubility, low bioavailability and less drug accumulation of chemotherapeutic drugs restrict its antitumor activities in clinic. DNA nanostructures are proposed as drug carriers due to their intrinsic biocompatibility and programmability. In this work, we demonstrate a novel DNA nanocarrier grafted with erlotinib as an effective drug delivery system (DDS) for anti-cancer treatment. Specifically, erlotinib (Er), a hydrophobic small molecule drug targeting the epidermal growth factor receptor (EGFR), is covalently conjugated with azide (N3) modified DNA strands and subsequently self-assembled on spatially programmable erlotinib-grafted 6 × 6 × 64 nt DNA nanostructures. Thus, Er was successfully grafted on DNA carriers and transformed into a hydrophilic formulation. The antitumor efficacy was evaluated both in vitro and in vivo, and enhanced cytotoxicity toward A549 cells and the marked inhibition of tumor growth for non-small-cell lung cancer (NSCLC) were observed.
中文翻译：
设计的厄洛替尼移植DNA纳米结构用于非小细胞肺癌治疗
在过去的20年中，一直采用化学疗法治疗非小细胞肺癌（NSCLC）。但是，水溶性差，生物利用度低和化学治疗药物的药物积累较少限制了其在临床上的抗肿瘤活性。DNA纳米结构因其固有的生物相容性和可编程性而被提议作为药物载体。在这项工作中，我们展示了一种新型的DNA纳米载体，其嫁接了厄洛替尼作为一种有效的抗癌药物递送系统（DDS）。具体来说，厄洛替尼（Er）是一种靶向表皮生长因子受体（EGFR）的疏水性小分子药物，与叠氮化物（N 3）修饰的DNA链，然后在空间可编程的厄洛替尼移植的6×6×64 nt DNA纳米结构上自组装。因此，Er成功地嫁接到了DNA载体上并转化为亲水性制剂。在体外和体内均评估了抗肿瘤功效，并观察到了对非小细胞肺癌（NSCLC）增强的A549细胞毒性和明显的肿瘤生长抑制作用。
更新日期：2020-11-27
中文翻译：
设计的厄洛替尼移植DNA纳米结构用于非小细胞肺癌治疗
在过去的20年中，一直采用化学疗法治疗非小细胞肺癌（NSCLC）。但是，水溶性差，生物利用度低和化学治疗药物的药物积累较少限制了其在临床上的抗肿瘤活性。DNA纳米结构因其固有的生物相容性和可编程性而被提议作为药物载体。在这项工作中，我们展示了一种新型的DNA纳米载体，其嫁接了厄洛替尼作为一种有效的抗癌药物递送系统（DDS）。具体来说，厄洛替尼（Er）是一种靶向表皮生长因子受体（EGFR）的疏水性小分子药物，与叠氮化物（N 3）修饰的DNA链，然后在空间可编程的厄洛替尼移植的6×6×64 nt DNA纳米结构上自组装。因此，Er成功地嫁接到了DNA载体上并转化为亲水性制剂。在体外和体内均评估了抗肿瘤功效，并观察到了对非小细胞肺癌（NSCLC）增强的A549细胞毒性和明显的肿瘤生长抑制作用。
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