Department of Chemistry, Istanbul Technical University, TR-34469 Istanbul, Turkey.
Department of Chemistry Technology, Mustafa Çıkrıkçıoğlu Vocational School, Kayseri University, TR-38280 Kayseri, Turkey.
Dalton Trans. 2022 May 17;51(19):7539-7550. doi: 10.1039/d2dt01033j.
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.
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。
