Synthesis, Structure, Electrochemistry, and Spectral Characterization of Bis-Isatin Thiocarbohydrazone Metal Complexes and Their Antitumor Activity Against Ehrlich Ascites Carcinoma in Swiss Albino Mice

The synthesis, structure, electrochemistry, and biological studies of Co(II), Ni(II), Cu(II), and Zn(II) complexes of thiocarbohydrazone ligand are described. The ligand is synthesized starting from thiocarbohydrazide and isatin. It is evident from the IR data that in all the complexes, only one part of the ligand is coordinated to the metal ion resulting mononuclear complexes. The ligand coordinates essentially through the carbonyl oxygen of the isatin fragment, the nitrogen atom of the azomethine group, and sulfur atom after deprotonation to give five membered rings. H1 NMR spectrum of the ligand shows only one set of signals for the aromatic protons, while the NH of isatin and NH of hydrazone give rise to two different singlets in the 11–14 ppm range. The formulations, [Cu(L)Cl]·2H2O, [Cu(L)(CH3COO)]·2H2O, [Ni(L)Cl], [Ni(L)(CH3COO)], [Co(L2)], and [Zn(L2)]·2H2O are in accordance with elemental analyses, physical, and spectroscopic measurements. The complexes are soluble in organic solvents. Molar conductance values in DMF indicate the nonelectrolytic nature of the complexes. Copper complex displays quasireversible cyclic voltametric responses with Ep near −0.659 v and 0.504 v Vs Ag/AgCl at the scan rate of 0.1 V/s. Copper(II) complexes show a single line EPR signals. For the observed magnetic moment and electronic spectral data possible explanation has been discussed. From all the available data, the probable structures for the complexes have been proposed. The compounds synthesized in present study have shown promising cytotoxic activity when screened using the in vitro method and at the same time were shown to have good activity when tested using the Ehrlich ascites carcinoma (EAC) model. The antimicrobial screening showed that the cobalt complex possesses enhanced antimicrobial activity towards fungi

Cytoprotective and antioxidant activity studies of jaggery sugar

Jaggery and other sugars namely white, refined and brown sugars were evaluated for cytoprotectivity on NIH 3T3 fibroblasts and erythrocytes, DPPH radical scavenging activity, reducing power and DNA protection. In addition, total phenol content and phenolic acid composition were also determined. Results indicated a total phenolic content of 26.5, 31.5, 372 and 3837 mu g GAE/g for refined, white, brown and jaggery, respectively. The HPLC analysis revealed the presence of different phenolic acids in brown sugar and jaggery. On NIH 3T3 cells oxidation, at 4 mg/ml concentration, jaggery showed 97% protection compared to brown sugar, and both Sugars effectively reduced erythrocyte oxidation. A dose dependent reducing power and DPPH radical scavenging activity was also observed for jaggery and brown sugar. An EC50 of 7.81 and 59.38 mu g/ml were observed for jaggery and brown sugar in the DPPH scavenging assay. In DNA oxidation studies, higher protection was observed in jaggery followed by brown, white and refined sugar treated samples. (C) 2008 Elsevier Ltd. All rights reserved

Synthesis and evaluation of Tricyclic Dipyrido Diazepinone derivatives as inhibitors of secretory Phospholipase A2 with Anti-Inflammatory activity

A series of tricyclic dipyrido diazepinone derivatives 6(a-f) bearing different substituents at the tenth position of diazepinone ring were designed and are characterized by 1H NMR, FTIR and X-Ray crystallography studies. The synthesised derivatives are tested in-vitro phospholipase A2 (PLA2) enzyme inhibitory activity and in-vivo antiinflammatory activity against purified group I and group II PLA2 enzymes from the snake venom and human pleural fluid. Compounds bearing aromatic ring with different substituents at different positions shown varied specificity. The 6f derivative with strong electron withdrawing nitro (-NO2) and trifluoromethyl (-CF3) groups at ortho and para positions respectively shown greater inhibitory activity. Inhibitory effect of the compound appeared to be direct interaction with active site and likely competes with substrates as supported by substrate dependent and calcium independent assays. The IC50 value of potent PLA2 inhibitor 6f was 22.1 μM and showed similar potency in the neutralization of in vivo PLA2 induced mouse paw edema and hemolytic activity