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聚乙二胺-环糊精-替加氟缀合物具有抗癌活性和基因传递的潜力。

Polyethylenimine-cyclodextrin-tegafur conjugate shows anti-cancer activity and a potential for gene delivery.

机构信息

Institute of Chemical Biology and Pharmaceutical Chemistry, Zhejiang University, Hangzhou, China.

出版信息

J Zhejiang Univ Sci B. 2011 Sep;12(9):720-9. doi: 10.1631/jzus.B1000307.

Abstract

Polyethylenimine-cyclodextrin-tegafur (PEI-CyD-tegafur) conjugate was synthesized as a novel multifunctional prodrug of tegafur for co-delivery of chemotherapeutic agent tegafur and enhanced green fluorescent protein (EGFP) reporter plasmid DNA. Conjugation of tegafur to PEI-CyD via chemical linkage was characterized by (1)H NMR spectrometry and ultraviolet (UV) spectrometry. PEI-CyD-tegafur was able to condense plasmid DNA into complexes of around 150 nm with positive charge at the N/P ratio of 25, in accordance with electron microscopy observation of compact and monodisperse nanoparticles. The results of in vitro experiments showed enhanced cytotoxicity and considerable transfection efficiency in B16F10 cell line. Therefore, PEI-CyD-tegafur may have great potential as a co-delivery system with anti-cancer activity and potential for gene delivery.

摘要

聚乙二醇化环糊精-替加氟(PEI-CyD-tegafur)缀合物被合成作为替加氟的新型多功能前药,用于共递送化疗药物替加氟和增强型绿色荧光蛋白(EGFP)报告质粒 DNA。通过化学连接将替加氟连接到 PEI-CyD 上,通过(1)H NMR 光谱和紫外(UV)光谱进行表征。PEI-CyD-tegafur 能够将质粒 DNA 凝聚成约 150nm 的复合物,在 N/P 比为 25 时带有正电荷,这与电子显微镜观察到的紧密和单分散纳米颗粒一致。体外实验结果表明,在 B16F10 细胞系中具有增强的细胞毒性和相当高的转染效率。因此,PEI-CyD-tegafur 可能作为具有抗癌活性和基因递送潜力的共递药系统具有巨大潜力。

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