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


Ontology type: schema:ScholarlyArticle     


Article Info

DATE

2019-03-30

AUTHORS

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

ABSTRACT

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. More... »

PAGES

1-8

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Identifiers

URI

http://scigraph.springernature.com/pub.10.1007/s10637-019-00765-9

DOI

http://dx.doi.org/10.1007/s10637-019-00765-9

DIMENSIONS

https://app.dimensions.ai/details/publication/pub.1113144038

PUBMED

https://www.ncbi.nlm.nih.gov/pubmed/30929158


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