Copper(II/I) complexes of 5-pyridin-2-yl-[1,3]dioxolo[4,5-g] isoquinoline: Synthesis, crystal structure, antitumor activity and DNA interaction
Copper(II/I) complexes of 5-pyridin-2-yl-[1,3]dioxolo[4,5-g] isoquinoline: Synthesis, crystal structure, antitumor activity and DNA interaction
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DOI：
10.1016/j.ejmech.2013.10.031
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发表时间：
2013-12-01
影响因子：
6.7
通讯作者：
Liang, Hong
中科院分区：
文献类型：
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作者：
Huang, Ke-Bin;Chen, Zhen-Feng;Liang, Hong
5-吡啶-2-基-[1,3]二氧杂环[4,5-g]异喹啉(PYP)的三个新铜(II)配合物，即[Cu-2(PYP)(2)Cl-4] (1)、[Cu-4(PYP)(4)(ClO4)(2)(H2O)(2)](ClO4)(2)中心点2H(2)O合成了 (2) 和 [Cu-2(PYP)(2)Cl-4](n) (3) 并进行了充分表征。与游离PYP相比，复合物1-3对测试的人肿瘤细胞系BEL-7404、SK-OV-3、A549、A375、MGC-803和NCI-H460表现出增强的细胞毒性，IC50值范围为0.31至30.76μM。复合物1-3对HL-7702的细胞毒性低于对癌细胞的细胞毒性。复合物 1 诱导 BEL-7404 凋亡，该过程涉及线粒体。 Caspase-3激活实验表明1可能是一种有效的caspase-3激活剂。通过 UV-vis、DNA 熔解、竞争性结合、CD、粘度测量和琼脂糖凝胶电泳进行的 DNA 结合研究表明，嵌入可能是 1 与 DNA 最可能的结合模式。 (C) 2013 Elsevier Masson SAS。版权所有。
Three new copper(II) complexes of 5-pyridin-2-yl-[1,3]dioxolo[4,5-g]isoquinoline (PYP), i.e. [Cu-2(PYP)(2)Cl-4] (1), [Cu-4(PYP)(4)(ClO4)(2)(H2O)(2)](ClO4)(2)center dot 2H(2)O (2), and [Cu-2(PYP)(2)Cl-4](n) (3), were synthesized and fully characterized. In comparison to free PYP, complexes 1-3 exhibited enhanced cytotoxicity against tested human tumor cell lines BEL-7404, SK-OV-3, A549, A375, MGC-803 and NCI-H460, with IC50 values ranging from 0.31 to 30.76 mu M. Complexes 1-3 exhibited lower cytotoxicity to HL-7702 than them to cancer cells. Complex 1 induced apoptotic death of BEL-7404, which involved mitochondria in the process. Caspase-3 activation assay indicated that 1 could be an efficient activator of caspase-3. DNA binding studies by UV-vis, DNA-melting, competitive binding, CD, viscosity measurement and agarose gel electrophoresis, revealed that intercalation might be the most likely binding mode of 1 with DNA. (C) 2013 Elsevier Masson SAS. All rights reserved.