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Cationic Polyrotaxanes Effectively Inhibit Uptake via Carnitine/Organic Cationic Transporters without Cytotoxicity
Author(s) -
Utsunomiya Hideto,
Katoono Ryo,
Yui Nobuhiko,
Sugiura Tomoko,
Kubo Yoshiyuki,
Kato Yukio,
Tsuji Akira
Publication year - 2008
Publication title -
macromolecular bioscience
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.924
H-Index - 105
eISSN - 1616-5195
pISSN - 1616-5187
DOI - 10.1002/mabi.200700297
Subject(s) - cationic polymerization , chemistry , cytotoxicity , organic cation transport proteins , ethylene glycol , transfection , peg ratio , transporter , hek 293 cells , biophysics , carnitine , biochemistry , in vitro , polymer chemistry , organic chemistry , receptor , biology , finance , economics , gene
We examined the inhibitory effect of cationic polyrotaxanes, which consist of α ‐cyclodextrins threaded on a poly(ethylene glycol) (PEG) chain, on the activity of the intestinal carnitine/organic cation transporter, OCTN2, in OCTN2 gene‐transfected HEK293/PDZK1 cells. The cationic polyrotaxanes effectively inhibited the OCTN2‐mediated carnitine transport. Polyrotaxanes with a longer PEG chain exhibited a greater inhibitory effect, possibly owing to multivalent interactions with binding sites on OCTN2. These cationic polyrotaxanes were far less cytotoxic than conventional polycations, and are therefore interesting candidates as low‐toxicity inhibitors of cation transport at cell surfaces.