DNA-binding, photocleavage, cytotoxicity in?vitro, apoptosis and cell cycle arrest studies of symmetric ruthenium(II) complexes

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• 作者：Yang-Yin Xie^a ; Hong-Liang Huang^c ; ^{hhongliang@163.com} ; Jun-Hua Yao^b ; Gan-Jian Lin^a ; Guang-Bin Jiang^a ; Yun-Jun Liu^a ; ^{lyjche@163.com}
• 关键词：Ruthenium(II) complexes ; DNA-binding ; Cytotoxicity ; Cellular uptake ; Cell cycle arrest
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2013
• 出版时间：May, 2013
• 年：2013
• 卷：63
• 期：Complete
• 页码：603-610
• 全文大小：2046 K

文摘

Two novel ruthenium(II) complexes [Ru(dmb)₂(addppn)](ClO₄)₂ (rong class=""boldFont"">1rong>) and [Ru(bpy)₂(addppn)](ClO₄)₂ (rong class=""boldFont"">2rong>) were synthesized. The DNA-binding constants of complexes rong class=""boldFont"">1rong> and rong class=""boldFont"">2rong> were determined to be 4.78 (¡À0.49)?¡Á?10⁵ and 7.42 (¡À0.53)?¡Á?10⁵?M^?1. The results indicate that complexes rong class=""boldFont"">1rong> and rong class=""boldFont"">2rong> interact with CT?DNA through intercalative mode. The cytotoxicity in?vitro of the complexes toward BEL-7402, HeLa, MG-63 and SKBR-3 cells was assessed by MTT assay. The apoptosis was carried out with Hoechst 33258 staining method and flow cytometry. The cellular uptake was observed under fluorescence microscope. The cell cycle arrest shows that the antiproliferative mechanism induced by complexes rong class=""boldFont"">1rong> and rong class=""boldFont"">2rong> on BEL-7402 cells is G0/G1 phase arrest.