Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, China.
Shandong Provincial Engineering Laboratory of Novel Pharmaceutical Excipients, Sustained and Controlled Release Preparations, College of Medicine and Nursing, Dezhou University, Dezhou 253023, China.
ACS Appl Mater Interfaces. 2020 Mar 4;12(9):10193-10201. doi: 10.1021/acsami.0c00652. Epub 2020 Feb 21.
Tumor targeting provided more effective gene therapy. Bcl-2 is an oncogene, and Bcl-2 small interfering RNA (Bcl-2 siRNA) can inhibit its expression. Here, a fluorescent and gene-loading capacity vector , derived from diketopyrrolopyrrole (DPP), was developed for Bcl-2 siRNA-targeted delivery and tumor imaging and . The vector showed a significant emission enhancement after interacting with siRNA, which was used to track the gene transfer process. Compared to commercial transfection reagent Lipo 2000, obviously downregulated the Bcl-2 protein expression and exhibited excellent antitumor efficacy with less Bcl-2 siRNA. Importantly, can target tumors to transport Bcl-2 siRNA to tumor sites based on the enhanced permeability and retention (EPR) effect for effective tumor therapy. This work inspired us to design and synthesize a multifunctional gene vector for tumor targeting and gene therapy.
肿瘤靶向提供了更有效的基因治疗。Bcl-2 是一种癌基因,Bcl-2 小干扰 RNA(Bcl-2 siRNA)可以抑制其表达。在这里,开发了一种荧光和基因负载能力载体,来源于二酮吡咯并吡咯(DPP),用于 Bcl-2 siRNA 的靶向递送和肿瘤成像。载体与 siRNA 相互作用后显示出显著的发射增强,可用于跟踪基因转移过程。与商业转染试剂 Lipo 2000 相比,明显下调了 Bcl-2 蛋白的表达,并表现出优异的抗肿瘤功效,所需 Bcl-2 siRNA 更少。重要的是,基于增强的通透性和保留(EPR)效应,能够靶向肿瘤将 Bcl-2 siRNA 输送到肿瘤部位,从而有效进行肿瘤治疗。这项工作启发我们设计和合成一种用于肿瘤靶向和基因治疗的多功能基因载体。