Multifunctional Hyperbranched
Glycoconjugated Polymers
Based on Natural Aminoglycosides
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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 <i>N</i>,<i>N</i>′-methylenebisacrylamide,
cationic hyperbranched glycoconjugated polymers were synthesized,
and their physical and chemical properties were analyzed by FTIR, <sup>1</sup>H NMR, <sup>13</sup>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