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钌(II)多吡啶配合物的合成及其与 DNA 的结合、光解、细胞毒性、细胞凋亡、细胞摄取和抗氧化活性的研究。

Ruthenium(II) polypyridyl complexes: synthesis and studies of DNA binding, photocleavage, cytotoxicity, apoptosis, cellular uptake, and antioxidant activity.

机构信息

School of Pharmacy, Guangdong Pharmaceutical University, Guangzhou, PR China.

出版信息

DNA Cell Biol. 2011 Oct;30(10):829-38. doi: 10.1089/dna.2010.1170. Epub 2011 Mar 13.

Abstract

Two ruthenium (II) complexes Ru(dmb)2(APIP)2 (APIP=2-(2-aminophenyl)imidazo[4,5-f ][1,10]phenanthroline, dmb=4,4'-dimethyl-2,2'-bipyridine; 1) and Ru(dmb)2(HAPIP)2 (HAPIP=2-(2-hydroxyl-4-aminophenyl)imidazo[4,5-f ][1,10]phenanthroline; 2) were synthesized and characterized. DNA binding was investigated by electronic absorption titration, luminescence spectra, thermal denaturation, viscosity measurements, and photocleavage. The DNA binding constants for complexes 1 and 2 were 4.20 (±0.14)×10(4) and 5.45 (±0.15)×10(4) M(-1). The results suggest that these complexes partially intercalate between the base pairs. The cytotoxicity of complexes 1 and 2 was evaluated by MTT assay. Cellular uptake was observed under fluorescence microscopy; complexes 1 and 2 can enter into the cytoplasm and accumulate in the nuclei. Apoptosis and the antioxidant activity against hydroxyl radicals (•OH) were also explored.

摘要

合成并表征了两个钌(II)配合物Ru(dmb)2(APIP)2(APIP=2-(2-氨基苯基)咪唑并[4,5-f][1,10]菲咯啉,dmb=4,4'-二甲基-2,2'-联吡啶;1)和Ru(dmb)2(HAPIP)2(HAPIP=2-(2-羟基-4-氨基苯基)咪唑并[4,5-f][1,10]菲咯啉;2)。通过电子吸收滴定、发光光谱、热变性、粘度测量和光解来研究 DNA 结合。配合物 1 和 2 的 DNA 结合常数分别为 4.20(±0.14)×10(4)和 5.45(±0.15)×10(4)M(-1)。结果表明这些配合物部分插入碱基对之间。通过 MTT 测定评估了配合物 1 和 2 的细胞毒性。在荧光显微镜下观察到细胞摄取;配合物 1 和 2 可以进入细胞质并在核内积累。还研究了细胞凋亡和对羟基自由基(•OH)的抗氧化活性。

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