School of Chemistry and Chemical Engineering, State Key Laboratory of Metal Matrix Composites, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai, 200240, P. R. China.
Angew Chem Int Ed Engl. 2017 Oct 2;56(41):12528-12532. doi: 10.1002/anie.201706301. Epub 2017 Sep 5.
Based on their structural similarity to natural nucleobases, nucleoside analogue therapeutics were integrated into DNA strands through conventional solid-phase synthesis. By elaborately designing their sequences, floxuridine-integrated DNA strands were synthesized and self-assembled into well-defined DNA polyhedra with definite drug-loading ratios as well as tunable size and morphology. As a novel drug delivery system, these drug-containing DNA polyhedra could ideally mimic the Trojan Horse to deliver chemotherapeutics into tumor cells and fight against cancer. Both in vitro and in vivo results demonstrate that the DNA Trojan horse with buckyball architecture exhibits superior anticancer capability over the free drug and other formulations. With precise control over the drug-loading ratio and structure of the nanocarriers, the DNA Trojan horse may play an important role in anticancer treatment and exhibit great potential in translational nanomedicine.
基于与天然核苷碱基的结构相似性，核苷类似物治疗剂通过传统的固相合成整合到 DNA 链中。通过精心设计它们的序列，合成了整合了氟尿嘧啶的 DNA 链，并自组装成具有确定载药比以及可调尺寸和形态的明确定义的 DNA 多面体。作为一种新型药物传递系统，这些含药 DNA 多面体可以理想地模拟特洛伊木马，将化疗药物递送到肿瘤细胞中并对抗癌症。体外和体内结果均表明，具有富勒烯结构的 DNA 特洛伊木马在抗癌能力方面优于游离药物和其他制剂。通过对纳米载体的载药比和结构进行精确控制，DNA 特洛伊木马可能在癌症治疗中发挥重要作用，并在转化纳米医学中具有巨大的潜力。
