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01-12-2019 | Breast Cancer | SHORT REPORT

Cellular uptake evaluation of pentagamaboronon-0 (PGB-0) for boron neutron capture therapy (BNCT) against breast cancer cells

Authors: Adam Hermawan, Ratna Asmah Susidarti, Ratna Dwi Ramadani, Lailatul Qodria, Rohmad Yudi Utomo, Miki Ishimura, Yoshihide Hattori, Yoichiro Ohta, Mitsunori Kirihata, Edy Meiyanto

Published in: Investigational New Drugs | Issue 6/2019

Summary

Pentagamaboronon-0 (PGB-0), a curcumin analog compound, has been synthesized as a candidate of boron-carrier pharmaceutical (BCP) for boron neutron capture therapy (BNCT); however, this compound is poorly soluble in water. To improve its solubility, aqueous formulations of PGB-0 with a monosaccharide, fructose or sorbitol, were successfully synthesized, namely PGB-0-F and PGB-0-So, respectively. The cytotoxicity study showed that PGB-0-F and PGB-0-So exerted low cytotoxicity against MCF-7 and MDA-MB 231 breast cancer cells. The cellular uptake study using inductively coupled plasma optical emission spectrometry (ICP-OES) and DAHMI live-cell imaging indicated that these compounds were accumulated and distributed within the cytoplasm and cell nuclei. The cellular uptake mechanism was also evaluated to clarify the contribution of the glucose transporter, and the results demonstrated that these compounds entered through active transport into MCF-7 cells but through passive diffusion into MDA-MB 231 cells. In conclusion, the sugar formulations of PGB-0 only improved PGB-0 solubility but had no role in its cellular uptake.

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Title: Cellular uptake evaluation of pentagamaboronon-0 (PGB-0) for boron neutron capture therapy (BNCT) against breast cancer cells
Authors: Adam Hermawan
Ratna Asmah Susidarti
Ratna Dwi Ramadani
Lailatul Qodria
Rohmad Yudi Utomo
Miki Ishimura
Yoshihide Hattori
Yoichiro Ohta
Mitsunori Kirihata
Edy Meiyanto
Publication date: 01-12-2019
Publisher: Springer US
Keywords: Breast Cancer
Breast Cancer
Published in: Investigational New Drugs / Issue 6/2019
Print ISSN: 0167-6997
Electronic ISSN: 1573-0646
DOI: https://doi.org/10.1007/s10637-019-00765-9

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