Evaluation of histone deacetylase inhibitor substituted zinc and indium phthalocyanines for chemo- and photodynamic therapy

In this study, we synthesized and characterized 3-hydroxypyridin-2-thione (3-HPT) bearing zinc ( ZnPc-1 and ZnPc-2 ) and indium ( InPc-1 and InPc-2 ) phthalocyanine (Pc) derivatives, either non-peripherally or peripherally substituted as photosensitizer (PS) agents and evaluated their anti-cancer ef...

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Bibliographic Details
Published in:RSC advances 2021-10, Vol.11 (55), p.34963-34978
Main Authors: Aru, Ba ak, Günay, Aysel, Demirel, Gülderen Yan kkaya, Gürek, Ay e Gül, Atilla, Devrim
Format: Article
Language:English
Subjects:
Anticancer properties
Cancer
Chemistry
Endothelial cells
Indium
Localization
Photodynamic therapy
Substitutes
Zinc
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Summary:In this study, we synthesized and characterized 3-hydroxypyridin-2-thione (3-HPT) bearing zinc ( ZnPc-1 and ZnPc-2 ) and indium ( InPc-1 and InPc-2 ) phthalocyanine (Pc) derivatives, either non-peripherally or peripherally substituted as photosensitizer (PS) agents and evaluated their anti-cancer efficacy on two breast cancer cell lines, MDA-MB-231 and MCF-7 as well as a human endothelial cell line, HUVEC. Our results indicated different localization patterns between ZnPcs and InPcs in addition to enhanced effects on the mitochondrial network for InPcs . Moreover, peripheral or non-peripheral substitution of HDACi moieties altered cellular localization between ZnPc-1 and ZnPc-2 , leading to increased IC 50 values along with decreased anti-cancer activity for non-peripheral substitution. When considering the compounds' differential effects in vitro , our data indicates that further research is required to determine the ideal Pcs for anti-cancer PDT treatments since the core metals of the compounds have affected the cellular localization, and positioning of the chemotherapeutic residues may inhibit cellular penetrance. 3-Hydroxypyridin-2-thione bearing zinc and indium phthalocyanine derivatives, as photosensitizer agents have been synthesized and evaluated for their anti-cancer efficacy on two breast cancer cell lines, MDA-MB-231 and MCF-7 as well as a human endothelial cell line, HUVEC.
ISSN:2046-2069
2046-2069
DOI:10.1039/d1ra05404j