Synthesis, Characterization, Interaction with DNA, and Cytotoxic Effect in Vitro of New Mono- and Dinuclear Pd(II) and Pt(II) Complexes with Benzo[d]thiazol-2-amine As the Primary Ligand

详细信息    查看全文

• 作者：EnJun Gao ; Lei Liu ; MingChang Zhu ; Yun Huang ; Feng Guan ; XiaNan Gao ; Min Zhang ; Lei Wang ; WanZhong Zhang ; YaGuang Sun
• 刊名：Inorganic Chemistry
• 出版年：2011
• 出版时间：June 6, 2011
• 年：2011
• 卷：50
• 期：11
• 页码：4732-4741
• 全文大小：1076K
• 年卷期：v.50,no.11(June 6, 2011)
• ISSN：1520-510X

文摘

A series of novel Pd(II) and Pt(II) complexes, [PdL₂Cl₂]路DMF (1), [Pd₂(L-H)₂(bpy)Cl₂]路(H₂O)₂路DMF (2), [Pd₂(L-H)₂(phen)Cl₂]路2H₂O (3), [PtL₂Cl₂]路H₂O (4), [Pt₂(L-H)₂(bpy)Cl₂]路2H₂O (5), and [Pt₂(L-H)₂(phen)Cl₂]路H₂O (6), where bpy = 2,2鈥?bipyridine, phen = 1,10-phenanthroline, and L = 1,3-benzothiazol-2-amine, have been synthesized and characterized. The competitive binding of the complexes to DNA has been investigated by fluorescence spectroscopy. The values of the apparent DNA binding constant, calculated from fluorescence spectral studies, were 3.8 脳 10⁶ (K_app(4)), 2.9 脳 10⁶ (K_app(1)), 2.4 脳 10⁶ (K_app(6)), 2.0 脳 10⁶ (K_app(5)), 1.2 脳 10⁶ (K_app(3)), and 6.9 脳 10⁵ (K_app(2)). The binding parameters for the fluorescence Scatchard plot were also determined. On the basis of the data obtained, it indicates that the six complexes bind to DNA with different binding affinities in the relative order 4 > 1 > 6 > 5 > 3 > 2. Viscosity studies carried out on the interaction of complexes with Fish Sperm DNA (FS-DNA) suggested that all complexes bind by intercalation. Gel electrophoresis assay demonstrates that all the complexes can cleave the pBR 322 plasmid DNA and bind to DNA in a similar mode. The cytotoxic activity of the complexes has been also tested against four different cancer cell lines. The results show that all complexes have activity against KB, AGZY-83a, Hep-G2, and HeLa cells. In general, the Pt(II) complexes were found to be more effective than the isostructural Pd(II) complexes. The mononuclear complexes exhibited excellent activity in comparison with the dinuclear complexes in these four cell lines. Moreover, on the KB cell line (the human oral epithelial carcinoma), the observed result seems quite encouraging for the six complexes with IC₅₀ values ranging from 1.5 to 8.6 渭M. Furthermore, apoptosis assay with hematoxylin鈥揺osin staining shows treatment with the six complexes results in morphological changes of KB cells. The results induce apoptosis in KB cells