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

Abstract

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.

Transcriptome Changes Associated with Boron Applications in Fruits of Watercore-susceptible Pear Cultivar

“…Moreover, boron has also been shown to form a stable complex with sorbitol and sucrose 17,18 . Although the function of boron in apple and pear remains unknown, it is becoming increasingly important to understand the signi cance of the formation of sorbitol-boron or sucrose-boron complexes in watercore development.…”