title: Tailoring the supramolecular structure of aminated polyrotaxanes toward enhanced cellular internalization.
abstract: The effects of the supramolecular polyrotaxane (PRX) structure on cellular internalization are investigated by flow cytometry and confocal laser scanning microscopy. AF-545-labeled aminated PRXs (APRXs) containing different numbers of threaded α-cyclodextrins (CDs) and amino groups are synthesized; their cellular uptakes are analyzed using HeLa cells in serum. The APRX threaded CD number is discovered to be a more critical factor for enhancing cellular internalization than the APRX amine content. Additionally, APRXs are demonstrated to be more easily internalized than conventional linear cationic macromolecules. Because increased numbers of threaded CDs are related to increased PRX rigidity, the PRX rigid frame resulting from CD molecules threaded on a poly(ethylene glycol) (PEG) chain is suitable for intracellular tools in therapy and diagnosis.
authors.affiliation: Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University, 2-3-10 Kanda-Surugadai, Chiyoda, Tokyo, 101-0062, Japan.
authors.forename: Nanako
authors.initials: N
authors.lastname: Yokoyama
authors.forename: Ji-Hun
authors.initials: JH
authors.lastname: Seo
authors.forename: Atsushi
authors.initials: A
authors.lastname: Tamura
authors.forename: Yoshihiro
authors.initials: Y
authors.lastname: Sasaki
authors.forename: Nobuhiko
authors.initials: N
authors.lastname: Yui
mesh_terms: D000586:Amination; D001692:Biological Transport; D002470:Cell Survival / Q000187:drug effects; D003505:Cyclodextrins / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D004337:Drug Carriers; D005456:Fluorescent Dyes / Q000737:chemistry; D006367:HeLa Cells; D006801:Humans; D015394:Molecular Structure; D020442:Poloxamer / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D011092:Polyethylene Glycols / Q000737:chemistry*; D043862:Rotaxanes / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D047391:alpha-Cyclodextrins / Q000737:chemistry*
chemical_list: D003505:Cyclodextrins; D004337:Drug Carriers; D005456:Fluorescent Dyes; D043862:Rotaxanes; D047391:alpha-Cyclodextrins; C475673:polyrotaxane; D020442:Poloxamer; D011092:Polyethylene Glycols
keywords: cellular internalization; cyclodextrin; electrostatic interaction; polyrotaxane; supramolecular structures