<i>closo</i>-Dodecaborate-conjugated human serum albumins: preparation and in vivo selective boron delivery to tumor

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  • Hiroyuki Nakamura
    Laboratory for Chemistry and Life Science , Institute of Innovative Research, Tokyo Institute of Technology , Yokohama, 226-8503 , Japan
  • Shunsuke Kikuchi
    Laboratory for Chemistry and Life Science , Institute of Innovative Research, Tokyo Institute of Technology , Yokohama, 226-8503 , Japan
  • Kazuki Kawai
    Laboratory for Chemistry and Life Science , Institute of Innovative Research, Tokyo Institute of Technology , Yokohama, 226-8503 , Japan
  • Satomu Ishii
    Laboratory for Chemistry and Life Science , Institute of Innovative Research, Tokyo Institute of Technology , Yokohama, 226-8503 , Japan
  • Shinichi Sato
    Laboratory for Chemistry and Life Science , Institute of Innovative Research, Tokyo Institute of Technology , Yokohama, 226-8503 , Japan

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<jats:title>Abstract</jats:title> <jats:p>Maleimide-functionalized <jats:italic>closo</jats:italic>-dodecaborate (MID) and isothiocyanate-functionalized <jats:italic>closo</jats:italic>-dodecaborate (ISD) were synthesized from <jats:italic>closo</jats:italic>-dodecaborate via ring opening reaction of 1,4-dioxane-<jats:italic>closo</jats:italic>-dedecaborate complex <jats:bold>1</jats:bold> with ammonia. MID was found to possess highest conjugation efficacy to bovine serum albumin among three <jats:italic>closo</jats:italic>-dodecaborate derivatives, MID, ISD, and <jats:bold>1</jats:bold>. The conjugation reaction of MID to human serum albumin (HSA) proceeded under PBS buffer conditions (pH 7.4). Boron distribution studies in colon 26 tumor-bearing mice revealed that HSA-MID was highly accumulated in tumor (23 ppm B), whereas boron concentrations in other organs such as liver, kidney and spleen were low (3~8 ppm B).</jats:p>

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