Aru Başak, Günay Aysel, Şenkuytu Elif, Yanıkkaya Demirel Gülderen, Gürek Ayşe Gül, Atilla Devrim
Department of Molecular Biology and Genetics, Gebze Technical University, 41400 Gebze, Kocaeli, Turkey.
Faculty of Medicine, Immunology Department, Yeditepe University, 34755 Ataşehir, İstanbul, Turkey.
ACS Omega. 2020 Oct 2;5(40):25854-25867. doi: 10.1021/acsomega.0c03180. eCollection 2020 Oct 13.
In this study, we synthesized and characterized a silicon phthalocyanine substituted with 3-hydroxypyridin-2-thione (), 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 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 . Our further studies will be conducted with primary breast cancer cell culture to give a better insight into the anticancer mechanism of the compound.
在本研究中,我们合成并表征了一种用3-羟基吡啶-2-硫酮取代的硅酞菁(),其设计为一种作为组蛋白脱乙酰酶抑制剂的化学光动力治疗剂,并且我们测定了其光物理、光化学和光生物学性质。接下来,我们评估了其对MCF-7、双阳性和MDA-MB-231、三阴性乳腺癌细胞系以及健康人内皮细胞系(HUVEC)的抗癌功效。我们的结果表明,由于其高单线态氧产率及其组蛋白脱乙酰酶下调特性, 可以靶向细胞的核仁,有效诱导细胞凋亡同时促进细胞周期停滞,表明对乳腺癌有强大的抗癌作用。我们将对原发性乳腺癌细胞培养进行进一步研究,以更好地了解该化合物的抗癌机制。