title: Multifunctional hyperbranched glycoconjugated polymers based on natural aminoglycosides.
abstract: 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'-methylenebisacrylamide, cationic hyperbranched glycoconjugated polymers were synthesized, and their physical and chemical properties were analyzed by FTIR, (1)H NMR, (13)C NMR, GPC, ζ-potential, and acid-base 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.
authors.affiliation: School of Chemistry and Chemical Engineering, State Key Laboratory of Metal Matrix Composites, Shanghai Jiao Tong University , 800 Dongchuan Road, Shanghai 200240, P. R. China.
authors.forename: Mingsheng
authors.initials: M
authors.lastname: Chen
authors.forename: Mei
authors.initials: M
authors.lastname: Hu
authors.forename: Dali
authors.initials: D
authors.lastname: Wang
authors.forename: Guojian
authors.initials: G
authors.lastname: Wang
authors.forename: Xinyuan
authors.initials: X
authors.lastname: Zhu
authors.forename: Deyue
authors.initials: D
authors.lastname: Yan
authors.forename: Jian
authors.initials: J
authors.lastname: Sun
mesh_terms: D000617:Aminoglycosides / Q000737:chemistry* / Q000494:pharmacology; D000818:Animals; D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology; D019556:COS Cells; D002470:Cell Survival / Q000187:drug effects; D002522:Chlorocebus aethiops; D004247:DNA / Q000008:administration & dosage*; D004926:Escherichia coli / Q000187:drug effects; D004927:Escherichia coli Infections / Q000188:drug therapy; D005839:Gentamicins / Q000737:chemistry* / Q000494:pharmacology; D006001:Glycoconjugates / Q000737:chemistry / Q000494:pharmacology; D006367:HeLa Cells; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy; D011108:Polymers / Q000737:chemistry* / Q000494:pharmacology; D014162:Transfection
chemical_list: D000617:Aminoglycosides; D000900:Anti-Bacterial Agents; D000970:Antineoplastic Agents; D005839:Gentamicins; D006001:Glycoconjugates; D011108:Polymers; D004247:DNA