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Gao E.,Shenyang University of Chemical Technology | Gao E.,International Key Laboratory of Shenyang Inorganic Molecule Based Chemistry | Guan F.,Shenyang University of Chemical Technology | Guan F.,International Key Laboratory of Shenyang Inorganic Molecule Based Chemistry | And 12 more authors.
Journal of Biological Inorganic Chemistry | Year: 2012

Two novel palladium(II) complexes with a thiosalicylic acid (HSC 6H 4CO 2H) ligand, with the formulas [Pd(TSA)(L)] ·mH 2O (TSA is thiosalicylic acid; in complex 1, L is 1,10-phenanthro line and m - 1; in complex 2, L is 2,2'-bipyridine and m - 2), have been synthesized and characterized. The coordination geometry of both palladium atoms is square planar; they are fourcoordinated and each is coordinated in an N,N,O -,S - mode. There is a sigmoid oxygen chain in complex 1, but an oxygen ring in complex 2. The competitive binding of the complexes to HeLa cell DNA (HL-DNA) has been investigated by fluorescence spectroscopy. The results show that the two complexes have the ability to bind with HL-DNA. Viscosity studies suggest that the complexes bind to DNA by intercalation. Gel electrophoresis assay demonstrated the ability of the complexes to cleave the HL-DNA. The two complexes exhibit cytotoxic specificity and a significant cancer cell inhibitory rate. The apoptosis tests indicated that the complexes have an apoptotic effect. Furthermore, complex 1 exhibits more biological activity than complex 2, which is mainly because the area of the aromatic ring of 1,10-phenanthroline is larger than that of 2,2'-bipyridine. © SBIC 2011. Source


Zhu M.,Shenyang University of Chemical Technology | Zhu M.,International Key Laboratory of Shenyang Inorganic Molecule Based Chemistry | He W.,Shenyang University of Chemical Technology | He W.,International Key Laboratory of Shenyang Inorganic Molecule Based Chemistry | And 14 more authors.
Life Sciences | Year: 2012

Aims: A bridging ligand 2,4,6-pyridine tricarboxylic acid (H 3ptc) and its manganese(II) complex [Mn(Hptc)(phen)(OH)]n(Hptc = 2,4,6-pyridine tricarboxylic acid, phen = 1,10-phenanthroline) have been synthesized and characterized. Main methods: The interaction with DNA (HeLa and KB) was carried out by fluorescence spectrum and gel electrophoresis assay. In vitro apoptosis assay and cytotoxicity assay detect the manganese (II) complex interaction with cancer cells. Key findings: Fluorescence spectrum demonstrated the ability of the complexes to interact with DNA in an intercalative mode. Gel electrophoresis assay exhibited more effective DNA-cleavage activity. In vitro apoptosis assay of the complexes were examined on HeLa and KB cells, exhibited cytotoxic specificity and a significant cancer cell inhibitory rate. Significance: The complex may be a latent antitumor agent as a result of its unique interaction mode with DNA and cancer cells inhibition effect. Source


Gao E.J.,Shenyang University of Chemical Technology | Gao E.J.,International Key Laboratory of Shenyang Inorganic Molecule Based Chemistry | Liu L.,Shenyang University of Chemical Technology | Liu L.,International Key Laboratory of Shenyang Inorganic Molecule Based Chemistry | And 16 more authors.
Inorganic Chemistry | Year: 2011

A series of novel Pd(II) and Pt(II) complexes, [PdL2Cl 2] · DMF (1), [Pd2(L-H)2(bpy)Cl 2] · (H2O)2 · DMF (2), [Pd 2(L-H)2(phen)Cl2] · 2H2O (3), [PtL2Cl2] · H2O (4), [Pt 2(L-H)2(bpy)Cl2] · 2H2O (5), and [Pt2(L-H)2(phen)Cl2] · H 2O (6), where bpy = 2,2'-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 × 106 (Kapp(4)), 2.9 × 106 (Kapp(1)), 2.4 × 106 (Kapp(6)), 2.0 × 106 (K app(5)), 1.2 × 106 (Kapp(3)), and 6.9 × 105 (Kapp(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 IC 50 values ranging from 1.5 to 8.6 μM. Furthermore, apoptosis assay with hematoxylin-eosin staining shows treatment with the six complexes results in morphological changes of KB cells. The results induce apoptosis in KB cells. © 2011 American Chemical Society. Source

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