合成结构明确的阳离子聚噻吩用于 DNA 结合和基因传递。
Synthesis of Structurally Defined Cationic Polythiophenes for DNA Binding and Gene Delivery.
机构信息
Department of Polymer Science & Engineering, School of Chemistry & Chemical Engineering, Nanjing University , Nanjing 210023, P. R. China.
School of Chemistry & Chemical Engineering, Shangqiu Normal University , Shangqiu 476000, P. R. China.
出版信息
ACS Appl Mater Interfaces. 2018 Feb 7;10(5):4519-4529. doi: 10.1021/acsami.7b17948. Epub 2018 Jan 24.
Water-soluble conjugated polymers (WCPs) have prospective applications in the field of bioimaging, disease diagnosis, and therapy. However, the use of WCPs with controllability and regioregularity for bioapplications have scarcely been reported. In this work, we synthesized polythiophenes containing ester side chains (P3ET) via Kumada catalyst-transfer polycondensation (KCTP) and confirmed a quasi-"living" chain-growth mechanism. In addition, we obtained cationic regioregular polythiophenes (cPTs) by aminolysis of P3ET with varied chain lengths, and studied DNA binding capability and gene delivery performance. Benefiting from photocontrolled generation of intracellular reactive oxygen species (ROS), the cationic polythiophenes successfully delivered DNA into tumor cells without additional polymer species.
水溶性共轭聚合物（WCPs）在生物成像、疾病诊断和治疗领域具有广阔的应用前景。然而，具有可控性和区域规整性的 WCPs 在生物应用中的报道却很少。在这项工作中，我们通过 Kumada 催化剂转移聚合法（KCTP）合成了含有酯侧链的聚噻吩（P3ET），并证实了一种准“活性”链增长机制。此外，我们通过 P3ET 的氨解反应得到了具有不同链长的阳离子规正聚噻吩（cPTs），并研究了其与 DNA 的结合能力和基因传递性能。得益于光控产生的细胞内活性氧（ROS），阳离子聚噻吩无需额外的聚合物种类即可成功将 DNA 递送至肿瘤细胞。
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