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Merck

A Translational Study of a Silicon Phthalocyanine Substituted with a Histone Deacetylase Inhibitor for Photodynamic Therapy.

ACS omega (2020-10-20)
Başak Aru, Aysel Günay, Elif Şenkuytu, Gülderen Yanıkkaya Demirel, Ayşe Gül Gürek, Devrim Atilla
RESUMEN

In this study, we synthesized and characterized a silicon phthalocyanine substituted with 3-hydroxypyridin-2-thione (SiPc-HDACi), designed to be a chemophotodynamic therapy agent acting as a histone deacetylase inhibitor, and we determined its photophysical, photochemical, and photobiological properties. Next, we evaluated its anticancer efficacy on MCF-7, double positive and MDA-MB-231, triple negative breast cancer cell lines, as well as on a healthy human endothelial cell line (HUVEC). Our results indicate that SiPc-HDACi can target nucleoli of cells, effectively inducing apoptosis while promoting cell cycle arrest thanks to its high singlet oxygen yield and its histone deacetylase downregulating properties, suggesting a powerful anticancer effect on breast cancer in vitro. Our further studies will be conducted with primary breast cancer cell culture to give a better insight into the anticancer mechanism of the compound.

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Sigma-Aldrich
Glutaraldehyde solution, 50 wt. % in H2O
Sigma-Aldrich
In Vitro Toxicology Assay Kit, Resazurin based
Sigma-Aldrich
Anticuerpo anti-mitocondrias, clon 113-1, conjugado Alexa Fluor 488, clone 113-1, from mouse, ALEXA FLUOR 488