TY - JOUR
T1 - Closo-Dodecaborate-conjugated human serum albumins
T2 - Preparation and in vivo selective boron delivery to tumor
AU - Nakamura, Hiroyuki
AU - Kikuchi, Shunsuke
AU - Kawai, Kazuki
AU - Ishii, Satomu
AU - Sato, Shinichi
N1 - Funding Information:
Acknowledgment: This work was supported by a Grant-in-Aid for Scientific Research (B) (No. 17H02202) from the Ministry of Education, Culture, Sports, Science and Technology, Japan and Terumo Foundation for Life Sciences and Arts.
Publisher Copyright:
© 2018 IUPAC & De Gruyter.
PY - 2018/3/28
Y1 - 2018/3/28
N2 - 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).
AB - 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).
KW - anticancer activity
KW - biomedical applications
KW - conjugation
KW - drug delivery
KW - IMEBORON-16
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U2 - 10.1515/pac-2017-1104
DO - 10.1515/pac-2017-1104
M3 - Article
AN - SCOPUS:85042008177
SN - 0033-4545
VL - 90
SP - 745
EP - 753
JO - Pure and Applied Chemistry
JF - Pure and Applied Chemistry
IS - 4
ER -