51. Dendrimeric Guanidinoneomycin for Cellular Delivery of Bio‐macromolecules
- Author
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Sganappa, Aurora, Wexselblatt, Ezequiel, Bellucci, Maria Cristina, Esko, Jeffrey D, Tedeschi, Gabriella, Tor, Yitzhak, and Volonterio, Alessandro
- Subjects
1.1 Normal biological development and functioning ,Underpinning research ,Generic health relevance ,Aminoglycosides ,Animals ,Biotin ,CHO Cells ,Carbocyanines ,Cell Survival ,Cricetinae ,Cricetulus ,Dendrimers ,Drug Carriers ,Endocytosis ,cellular uptake ,dendrimers ,drug delivery ,guanidinium-rich transporters ,guanidinoglycosides ,PAMAM ,Medicinal and Biomolecular Chemistry ,Biochemistry and Cell Biology ,Organic Chemistry - Abstract
We present the synthesis of polymeric amino- and guanidinoglycosides prepared by tethering neomycin and guanidinoneomycin to PAMAM dendrimers of generations 2 and 4. The ability of these conjugates to promote cellular uptake of high-molecular-weight cargo is discussed, together with their cytotoxicity and mechanisms of entry. We demonstrate that the presence of multiple guanidinoneomycin carriers on the PAMAM surface plays an important role in promoting cellular uptake of the dendrimers, maintaining the heparan sulfate specificity and negligible cytotoxicity typical of monomeric guanidinoglycoside molecular transporters.
- Published
- 2017