Tianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics (Theranostics), School of Pharmacy, Tianjin Medical University, Tianjin, P. R. China.
Key Laboratory of Advanced Energy Materials Chemistry (Ministry of Education), Nankai University, Tianjin, P. R. China.
J Biomol Struct Dyn. 2020 Feb;38(3):733-743. doi: 10.1080/07391102.2019.1587511. Epub 2019 Mar 26.
Three dinuclear lanthanide complexes, [Ln(L)(μ-OAc)(HO)]⋅2HO (Ln = La (), Eu () and Dy (), HL = N'-(2-hydroxybenzylidene) nicotinohydrazide), have been synthesized and characterized by IR, elemental analysis and X-ray single-crystal diffraction. Crystallographic study revealed that the representative complex displays a discrete dinuclear structure with a distorted tricapped trigonal prismatic geometry around La(III) ion. The interaction of complexes - with CT-DNA was investigated by absorption spectra, fluorescence quenching and viscosity, which reveals that the complexes bind to CT-DNA with a moderate intercalative mode. The complexes exhibited obvious DNA cleavage activities in the presence of HO. All complexes could bind to human serum albumin (HSA) with medium affinity through static mode; thus, HSA could effectively transport complexes. Furthermore, three complexes exhibited specific cytotoxicity to A549 cancer cells in micromole magnitude than other cancer cells tested and less toxicity than cisplatin for normal human cells HUVEC, in which massive cell apoptosis was induced by complexes through producing DNA damage and suppressing DNA synthesis.Communicated by Ramaswamy H. Sarma.
三种双核镧系元素配合物,[Ln(L)(μ-OAc)(HO)]⋅2HO(Ln = La (),Eu () 和 Dy (),HL = N'-(2-羟基苯亚甲基)烟酰腙),已经通过红外光谱、元素分析和 X 射线单晶衍射进行了合成和表征。晶体学研究表明,代表性配合物 显示出离散的双核结构,镧(III)离子周围具有扭曲的三角双锥几何形状。通过吸收光谱、荧光猝灭和粘度研究了配合物 - 与 CT-DNA 的相互作用,结果表明配合物以适度的嵌入模式与 CT-DNA 结合。在 HO 的存在下,配合物表现出明显的 DNA 切割活性。所有配合物都可以通过静态模式与人血清白蛋白(HSA)以中等亲和力结合;因此,HSA 可以有效地转运配合物。此外,三种配合物对 A549 癌细胞的细胞毒性在微摩尔量级上明显高于其他测试的癌细胞,对正常人脐静脉内皮细胞(HUVEC)的毒性低于顺铂,配合物通过产生 DNA 损伤和抑制 DNA 合成诱导大量细胞凋亡。由 Ramaswamy H. Sarma 通讯。