Improvement of BNCT effect by control of intracellular distribution

曲酸对黑素细胞具有增白作用。这一事实表明曲酸可以作为黑色素瘤靶向的有效配体。我们使用曲酸-碳硼烷共轭物（CKA）。由于CKA显示出很小的水溶性，因此使用各种环糊精作为增溶剂。由于羟丙基-β-环糊精（HP-b-CD）的包合复合物提供了最高浓度的CKA溶液，因此在本文中，CKA/HP-b-CD复合物被估计为用于黑素瘤靶向BNCT的硼载体。在B16 BL 6细胞中，CKA被有趣地定位于细胞核。当使用1500 ppm的10 B溶液时，使用L-BPA/果糖和CKA/HP-b-CD复合物的平均存活率分别为19天和22天。此外，用4500 ppm的CKA/HP-b-CD复合物的10 B溶液观察到长的存活率（25天）。加曲酸的碳硼烷有望成为治疗黑色素瘤BNCT的有效硼剂。

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.