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-Nezhad (2013) Pyrimidine-fused heterocycle derivatives as a novel class of inhibitors for α-glucosidase,

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There are several evidences, suggesting a relationship between hyperhomocysteinemia and various diseases of the visual system. Therefore in this study the effects of homocysteinylation on aggregation and fibrillation of lens crystallins were studied using spectroscopic techniques, SDS-PAGE and western blot analysis. The results of UV-Vis absorption studies suggest an induction of lens protein aggregation after homocysteinylation. Furthermore, the existence of fibril in the aggregate of lens proteins confirmed by Congo red absorption measurement and Thioflavin-T fluorescence assay. Taken together the results of SDS-PAGE and Western blotting, it is suggested that almost all detectable eye lens crystallins are prone to aggregation by homocysteinylation, while α-Crystallin comprises the main portion of lens protein aggregate. Overall this study may suggest lens protein homocysteinylation as a possible mechanism to explain the relationship between hyperhomocysteinimia and some impairments of the visual system.

The two six-coordinate Pt(IV) complexes, containing bidentate nitrogen donor/methyl ligands with general formula [Pt(X)2Me2((t)bu2bpy)], where (t)bu2bpy = 4,4'-ditert-butyl-2,2'-bipyridine and X = Cl (C1) or Br (C2), serving as the leaving groups were synthesized for evaluation of their anticancer activities and DNA binding properties. To examine anticancer activities of the synthetic complexes, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay and ethidium bromide/acridine orange (EB/AO) staining method were performed. The binding properties of these complexes to DNA and purine nucleotides were examined, using different spectroscopic techniques. These complexes demonstrated significant anticancer activities against three cancer cell lines Jurkat, K562, and MCF-7. On the basis of the results of EB/AO staining, C1 and C2 were also capable to induce apoptosis in cancer cells. These complexes comprise halide leaving groups, displaying different departure rates; accordingly, they demonstrated slightly dissimilar anticancer activity and significantly different DNA/purine nucleotide binding properties. The results of DNA interaction studies of these complexes suggest a mixed-binding mode, comprising partial intercalation and groove binding. Overall, the results presented herein indicate that the newly synthesized Pt(IV) complexes are promising class of the potential anticancer agents which can be considered as molecular templates in designing novel platinum anticancer drugs. This study also highlights the importance of leaving group in anticancer activity and DNA binding properties of Pt(IV) complexes.

Densities and speeds of sound for the pure as well as binary mixtures of 1,2-butanediol and benzyl alcohol, 2-phenylethanol, 2-butanol, and 1,3-butanediol were measured over the 0 to 1 composition range and at six different temperatures between 298.150 K and 323.150 K with an interval of 5 K and at atmospheric pressure using a vibrating tube densimeter.The experimental values were used to calculate excess molar volume, V m E , excess isentropic compressibility, K S E , excess thermal expansion coefficient, α p E , infinite partial molar volumes, V̅ i ∞ and excess partial molar volumes at infinite dilution, V̅ i E,∞ . The sign and magnitude of mixing quantities have been used to discuss the nature and strength of molecular interactions in binary mixtures. The calculated excess values and deviation quantities were fitted to the Redlich−Kister polynomials equation. Furthermore, it has been checked how the calculated values of densities and excess molar volumes using the Tao−Mason equation of state compare with the experimental ones.

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