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

• Main Authors: Ratna Asmah Susidarti (Author), Rohmad Yudi Utomo (Author), Lailatul Qodria (Author), Ratna Dwi Ramadani (Author), Youichiro Ohta (Author), Yoshihide Hattori (Author), Mitsunori Kirihata (Author), Edy Meiyanto (Author)
• Format: Book
• Published: Wolters Kluwer Medknow Publications, 2019-01-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.
• Notes: 1735-5362; 1735-9414; 10.4103/1735-5362.263552
• Keywords: bnct; boron carrier; fructose and sorbitol complexes; pgb-0; Pharmacy and materia medica; RS1-441
• Source: Research in Pharmaceutical Sciences, Vol 14, Iss 4, Pp 286-292 (2019)

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.