State Key Laboratory of Structural Chemistry, Fujian Institute of Research on the Structure of Matter, Chinese Academy of Sciences, Fuzhou 350002, PR China.
Key Laboratory of Biomedical Polymers of Ministry of Education, Department of Chemistry, Wuhan University, Wuhan 430072, PR China.
Biomaterials. 2014 Feb;35(6):2039-50. doi: 10.1016/j.biomaterials.2013.11.034. Epub 2013 Dec 4.
Myo-Inositol (INO) is a biomolecule with crucial functions in many aspects. In this study, hyperbranched copolymers for gene delivery were synthesized based on inositol and low molecular weight polyethylenimine. The capacity of INO-PEIs to load plasmid DNA and their biocompatibility was demonstrated. A tumor target ligand, folic acid (FA), which was widely used for drug delivery systems, was subsequently conjugated to INO-PEIs and resulted in INO-PEI-FA copolymers. The polymers were then evaluated on their activity to mediate transgene expression in mammalian cell lines. As indicated, INO-PEIs were able to mediate efficient transgene expression, which was particularly noticeable in carcinoma cell line HeLa. INO-PEI-FA further improved the efficiency in HepG2. Distribution of INO-PEI-FA polymers in non-carcinoma NIH 3T3 and carcinoma HeLa cell lines was discussed.
肌醇（INO）是一种在许多方面具有关键功能的生物分子。在这项研究中，基于肌醇和低分子量聚乙烯亚胺合成了用于基因传递的超支化共聚物。证明了 INO-PEI 负载质粒 DNA 的能力及其生物相容性。随后，将肿瘤靶配体叶酸（FA）与 INO-PEI 缀合，得到 INO-PEI-FA 共聚物，FA 广泛用于药物传递系统。然后评估聚合物在介导哺乳动物细胞系中转基因表达的活性。结果表明，INO-PEI 能够介导有效的转基因表达，在癌细胞系 HeLa 中尤为明显。INO-PEI-FA 进一步提高了 HepG2 的效率。讨论了 INO-PEI-FA 聚合物在非癌细胞系 NIH 3T3 和癌细胞系 HeLa 中的分布。
