Closo-Dodecaborate-conjugated human serum albumins: Preparation and in vivo selective boron delivery to tumor

Hiroyuki Nakamura, Shunsuke Kikuchi, Kazuki Kawai, Satomu Ishii, Shinichi Sato

Research output: Contribution to journalArticlepeer-review

6 Citations (Scopus)


Maleimide-functionalized closo-dodecaborate (MID) and isothiocyanate-functionalized closo-dodecaborate (ISD) were synthesized from closo-dodecaborate via ring opening reaction of 1,4-dioxane-closo-dedecaborate complex 1 with ammonia. MID was found to possess highest conjugation efficacy to bovine serum albumin among three closo-dodecaborate derivatives, MID, ISD, and 1. 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).

Original languageEnglish
Pages (from-to)745-753
Number of pages9
JournalPure and Applied Chemistry
Issue number4
Publication statusPublished - 2018 Mar 28
Externally publishedYes


  • anticancer activity
  • biomedical applications
  • conjugation
  • drug delivery

ASJC Scopus subject areas

  • Chemistry(all)
  • Chemical Engineering(all)


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