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新型轴向取代硅酞菁的抗癌和生物特性。

Anticancer and biological properties of new axially disubstituted silicon phthalocyanines.

机构信息

Department of Chemistry, Istanbul Technical University, TR-34469 Istanbul, Turkey.

Department of Chemistry Technology, Mustafa Çıkrıkçıoğlu Vocational School, Kayseri University, TR-38280 Kayseri, Turkey.

出版信息

Dalton Trans. 2022 May 17;51(19):7539-7550. doi: 10.1039/d2dt01033j.

Abstract

This study reports the synthesis of three novel axially disubstituted silicon phthalocyanines (1-3-Si) and their quaternized phthalocyanines (1-3-QSi). The resulting compounds were characterized by applying spectroscopic techniques including H NMR, FT-IR, UV-vis, and mass spectroscopy. The biological properties of compounds 1-3-QSi, including DNA cleavage activities, DNA binding modes, and topoisomerase enzyme inhibition activities, were investigated using agarose gel electrophoresis. pBR322 plasmid DNA, CT-DNA, and AL-DNA (isolated from apricot leaf) were used for DNA studies. All the quaternized compounds exhibited acceptable DNA cleavage activities. Human topoisomerase I and topoisomerase enzymes were used for the topoisomerase I inhibition studies. All the quaternized complexes inhibited topoisomerase I activity. Moreover, these compounds were screened for cytotoxic and apoptotic effects against a human colon cancer cell line (DLD-1) by performing MTT and Annexin V assays. They exhibited toxicity and apoptotic effect on the DLD-1 cell line. The findings reveal that the compounds can be utilized for cancer therapy after further investigations.

摘要

本研究报告了三种新型轴向取代硅酞菁(1-3-Si)及其季铵化酞菁(1-3-QSi)的合成。通过应用包括 H NMR、FT-IR、UV-vis 和质谱在内的光谱技术对所得化合物进行了表征。使用琼脂糖凝胶电泳研究了化合物 1-3-QSi 的生物学性质,包括 DNA 断裂活性、DNA 结合模式和拓扑异构酶抑制活性。pBR322 质粒 DNA、CT-DNA 和 AL-DNA(从杏叶中分离得到)用于 DNA 研究。所有季铵化化合物均表现出可接受的 DNA 断裂活性。人拓扑异构酶 I 和拓扑异构酶酶用于拓扑异构酶 I 抑制研究。所有季铵化配合物均抑制拓扑异构酶 I 活性。此外,通过 MTT 和 Annexin V 测定法对这些化合物进行了人结肠癌细胞系(DLD-1)的细胞毒性和凋亡作用筛选。它们对 DLD-1 细胞系表现出毒性和凋亡作用。研究结果表明,这些化合物在进一步研究后可用于癌症治疗。

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