Reduction-responsive multifunctional hyperbranched polyaminoglycosides with excellent antibacterial activity, biocompatibility and gene transfection capability

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• 作者：Yajun Huang^a ; ^b ; ^c ; ¹ ; Xiaokang Ding^a ; ^b ; ^c ; ¹ ; Yu Qi^a ; ^b ; ^c ; Bingran Yu^a ; ^b ; ^c ; ^{yubr@mail.buct.edu.cn" class="auth_mail" title="E-mail the corresponding author} ; Fu-Jian Xu^a ; ^b ; ^c ; ^{xufj@mail.buct.edu.cn" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Aminoglycoside ; Hyperbranched polymer ; Reduction-responsive ; Antibacterial ; Gene vectors
• 刊名：Biomaterials
• 出版年：2016
• 出版时间：November 2016
• 年：2016
• 卷：106
• 期：Complete
• 页码：134-143
• 全文大小：3868 K

文摘

There is an increasing demand in developing of multifunctional materials with good antibacterial activity, biocompatibility and drug/gene delivery capability for next-generation biomedical applications. To achieve this purpose, in this work series of hydroxyl-rich hyperbranched polyaminoglycosides of gentamicin, tobramycin, and neomycin (HP and SS-HP with redox-responsive disulfide bonds) were readily synthesized via ring-opening reactions in a one-pot manner. Both HP and SS-HP exhibit high antibacterial activity toward Escherichia coli and Staphylococcus aureus. Meanwhile, the hemolysis assay of the above materials shows good biocompatibility. Moreover, SS-HPs show excellent gene transfection efficiency in vitro due to the breakdown of reduction-responsive disulfide bonds. For an in vivo anti-tumor assay, the SS-HP/p53 complexes exhibit potent inhibition capability to the growth of tumors. This study provides a promising approach for the design of next-generation multifunctional biomedical materials.