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Abstract: Four novel Zn(II) complexes [Zn(L1)(bipy)(H2O)2]·4H2O(1), [Zn(L1)(phen)(H2O)2]·4H2O(2), [Zn(L2)(bipy)(H2O)2]·4H2O(3) and [Zn(L2)(phen)(H2O)2]·4H2O (4), where bipy=2,2′-bipyridine, phen=1,10-phenanthroline, L1 =2,2′-bipyridine 5,5′-dicarboxylic acid, L2 =2,2′-bipyridine-4,4′-dicarboxylic acid, have been synthesized and characterized using IR, 1H NMR, element analysis and single-crystal X-ray diffractometry. The unit cell parameters for the title complex (1), a =7.9621(10)Å, b =12.6853(17)Å, c =13.3714(17)Å, α =68.549(2)°, β=79.065(2)°, γ =88.723(2)°, V =1232.5(3)Å3, Z =15, space group,P-1(2).complex (4) a =9.5710(5)Å, b =14.1140(7)Å, c =19.0045(9)Å, α =90°, β =99.9920(10)°, γ =90°, V =2528.3(2)Å3, Z =32, space group, P121/n 1(14). The binding of the complexes with fish sperm DNA (FS-DNA) was investigated by electronic absorption spectra and fluorescence spectroscopy, showing that the complexes have the ability of interaction with DNA of intercalative mode. The intrinsic binding constant K of the complexes with FS-DNA is 0.37×105 M−1 (1) 0.73×105 M−1 (2), 0.98×105 M−1 (3), and 1.05×105 M−1 (4). The results indicate that the four complexes bound to DNA with different binding affinity, in the order complex 4 > 3 > 2 > 1. Gel electrophoresis assay demonstrates the ability of the complexes to cleave the pBR322 plasmid DNA. The cytotoxic activity of the complexes was tested against four different cancer cell lines. The four complexes exhibited cytotoxic specificity and significant cancer cell inhibitory rate. [Copyright &y& Elsevier]

Abstract: Two novel complexes, namely, [Pd(pdc)2]·(dmp)·6H2O (1) and [Pd(pdc)2K(H2O)5·3H2O]n (2) [H2pdc=pyridine-2,3-dicarboxylate acid, dmp=2,9-Dimethyl-1,10-phenanthroline] were synthesized and characterized as pH-dependent products. Gel electrophoresis assay demonstrated the ability of the complexes to cleave the pBR 322 plasmid DNA. Values of IC50 calculated for complexes 1 and 2 show that the two complexes exhibit good cytotoxic activity against different cell lines tested in general, especially more effective against HL-60 and A2780cisR cell lines. [Copyright &y& Elsevier]

Sishen Wan (SSW) is a commercial and frequently used Chinese patent medicine listed in the Chinese Pharmacopeia, which is usually used to treat chronic colitis. We explored the pharmacological mechanism of Sishen Wan attenuated experimental chronic colitis by inhibiting Wnt/β-catenin pathway. Experimental chronic colitis was induced by trinitrobenzene sulfonic acid (TNBS). The therapeutic effect of SSW were analyzed by index of colonic weight, colonic length, pathological score. Cytokines expression were analyzed by ELISA, while the apoptosis level was checked by TUNEL staining. These proteins of Wnt/β-catenin signaling pathway was analyzed by Western blot assay. Rats with TNBS-induced chronic colitis were treated by SSW for 10 days. The efficacy of SSW was demonstrated by improved macroscopic and microscopic colonic damage. SSW increased the level of ATP in colonic mucosa, while SSW inhibited β-catenin, ubiquitination of Nemo-like-kinase-associated ring finger protein and T-cell factor, and expression of Wnt/β-catenin downstream proteins (including c-Myc, cyclo-oxygenase-2, cyclin D1, survivin, signal transducer and activator of transcription 3 and zipper-interacting protein kinase), and improved lymphoid enhancer factor ubiquitination and β-TrCP activity, followed by excessive apoptosis of colonic epithelial cells. SSW effectively attenuated experimental chronic colitis induced by TNBS, which was realized by inhibition of the Wnt/β-catenin signaling pathway. Image 1 [ABSTRACT FROM AUTHOR]