Improvement of BNCT effect by control of intracellular distribution

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Kojic acid possesses a whitening ability to melanocytes. This fact suggests that kojic acid could work as effective ligand for melanoma-targeting. We used kojic acid-carborane conjugate (CKA). Because CKA shows little water-solubility, various cyclodextrins were used as a solubilizer. As the inclusion complex of hydroxypropyl-beta-cyclodextrin (HP-b-CD) provided the highest concentration of CKA solution, herein, the CKA/HP-b-CD complex was estimated as a boron carrier for melanoma-targeting BNCT. In B16BL6 cells, CKA was interestingly localized in the nucleus. When 1500 ppm of 10B solutions were used, average survival rate were 19 and 22 days with L-BPA/fructose and CKA/HP-b-CD complex, respectively. Moreover, long survival rates (25 days) were observed with 4500 ppm of 10B solutions of CKA/HP-b-CD complex. Kojic ac-id-appended carborane is promising to be an efficient boron agent toward melanoma BNCT.