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ORIGINAL ARTICLE
Year : 2019  |  Volume : 14  |  Issue : 4  |  Page : 286-292

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


1 Department of Pharmaceutical Chemistry; Cancer Chemoprevention Research Center, Faculty of Pharmacy, Universitas Gadjah Mada, Yogyakarta, Indonesia, 55281., Indonesia
2 Cancer Chemoprevention Research Center, Faculty of Pharmacy, Universitas Gadjah Mada, Yogyakarta, Indonesia, 55281, Indonesia
3 Research Center of Boron Neutron Capture Therapy, Research Organization for the 21st Century, Osaka Prefecture University, 1-1 Gakuen-cho, Nakaku, Sakai, Osaka, Japan

Correspondence Address:
Edy Meiyanto
Department of Pharmaceutical Chemistry; Cancer Chemoprevention Research Center, Faculty of Pharmacy, Universitas Gadjah Mada, Yogyakarta
Indonesia
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Source of Support: None, Conflict of Interest: None


DOI: 10.4103/1735-5362.263552

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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.


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