Preparation of pentagamaboronon-0 and its fructose and sorbitol complexes as boron carrier for boron neutron capture therapy (BNCT) applicatio

Ratna Asmah Susidarti , Rohmad Yudi Utomo, Lailatul Qodria, Ratna Dwi Ramadani, Youichiro Ohta, Yoshihide Hattori, Mitsunori Kirihata, Edy Meiyanto


Development of specific and selective boron carriers is indispensable for boron neutron capture therapy (BNCT) application. Pentagamaboronon-0 (PGB-0) is a promising candidate as boron carrier compound  due to the low but selective cytotoxicity in breast cancer cells. Formerly we reported synthesis of PGB-0 which was ineffective due to its low aqueous solubility. In the present study, we, therefore, introduced  the new PGB-0 preparation complexed with sugars to increase its solubility in water. By synthesizing  at room temperature and using flash chromatography for the purification, we produced PGB-0 with a yield of 40%. PGB-0 fructose complex (PGB-0-F) and PGB-0 sorbitol complex (PGB-0-Sor)  were obtained with smaller particle size compared to PGB-0 suspension in water. Based on the MTT assay, the cytotoxicity of PGB-0-F and PGB-0-Sor were higher than PGB-0 even though still categorized  as low cytotoxic agents. In conclusion, we provided PGB-0 with a new method and improved its solubility in water. Further investigations are still needed to develop more efficient PGB-0 as boron carrier  for BNCT in various cancers.


BNCT; Boron carrier; Fructose and sorbitol complexes; PGB-0.

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