Multifunctional Hyperbranched Glycoconjugated Polymers Based on Natural Aminoglycosides

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• 作者：Mingsheng Chen ; Mei Hu ; Dali Wang ; Guojian Wang ; Xinyuan Zhu ; Deyue Yan ; Jian Sun
• 刊名：Bioconjugate Chemistry
• 出版年：2012
• 出版时间：June 20, 2012
• 年：2012
• 卷：23
• 期：6
• 页码：1189-1199
• 全文大小：615K
• 年卷期：v.23,no.6(June 20, 2012)
• ISSN：1520-4812

文摘

Multifunctional gene vectors with high transfection, low cytotoxicity, and good antitumor and antibacterial activities were prepared from natural aminoglycosides. Through the Michael-addition polymerization of gentamycin and N,N鈥?methylenebisacrylamide, cationic hyperbranched glycoconjugated polymers were synthesized, and their physical and chemical properties were analyzed by FTIR, ¹H NMR, ¹³C NMR, GPC, 味-potential, and acid鈥揵ase titration techniques. The cytotoxicity of these hyperbranched glycoconjugated polycations was low because of the hydrolysis of degradable glycosidic and amide linkages in acid conditions. Owing to the presence of various primary, secondary, and tertiary amines in the polymers, hyperbranched glycoconjugated polymers showed high buffering capacity and strong DNA condensation ability, resulting in the high transfection efficiency. In the meantime, due to the introduction of natural aminoglycosides into the polymeric backbone, the resultant hyperbranched glycoconjugated polymers inhibited the growth of cancer cells and bacteria efficiently. Combining the gene transfection, antitumor, and antibacterial abilities together, the multifunctional hyperbranched glycoconjugated polymers based on natural aminoglycosides may play an important role in protecting cancer patients from bacterial infections.