Cationic Polyrotaxanes Effectively Inhibit Uptake via Carnitine/Organic Cationic Transporters without Cytotoxicity

✍ Scribed by Hideto Utsunomiya; Ryo Katoono; Nobuhiko Yui; Tomoko Sugiura; Yoshiyuki Kubo; Yukio Kato; Akira Tsuji

• Book ID: 102472946
• Publisher: John Wiley and Sons
• Year: 2008
• Tongue: English
• Weight: 201 KB
• Volume: 8
• Category: Article
• ISSN: 1616-5187
• DOI: 10.1002/mabi.200700297

✦ Synopsis

Abstract

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.

magnified image