Synthesis, structural characterization and biological properties of cyclometalated iridium(iii) complexes containing 1,2,5]-thiadiazolo-3,4-f]-1,10]-phenanthroline

Two cationic iridium(iii) complexes, Ir(ppy)(2)((tdzp))](+)(1) and Ir(bhq)(2)((tdzp))](+)(2) {ppy = 2-phenylpyridine, bhq = benzoh]quinoline, tdzp = 1,2,5]-thiadiazolo-3,4-f]-1,10]-phenanthroline}, have been synthesized and structurally characterized. The molecular structures of the iridium complexes have been confirmed by single-crystal X-ray structure determination. Extensive hydrogen bonding between lattice water molecules, solvated methanol, and chloride anions is observed in the crystal structure of complex1, which leads to the formation of 1D polymeric cyclic hybrid water-chloride-methanol clusters. The complexes show different photophysical properties in different solvents. The experimental photo-physical properties of the synthesized iridium(iii) complexes match well with the theoretically calculated results obtained by density functional theory (DFT) and time-dependent density functional theory (TD-DFT) studies. The HOMO of complexes1and2is restricted on the iridium and cyclometalated aromatic ligands, while the LUMO, LUMO+1, and LUMO+2 are primarily restricted on the polypyridyl tdzp ligand. The interaction of the complexes with calf thymus DNA (CT-DNA) was investigated by absorption titration and emission titration experiments. Furthermore, the cytotoxicity and cellular localization properties of these complexes towards HeLa cells have been investigated

Fluorophore tagged mixed ligand copper(II) complexes: synthesis, structural characterization, protein binding, DNA cleavage and anticancer activity

Two fluorophore tagged copper(II) complexes Cu(phen)(L)(ClO4)(2)] (1) and Cu(bpy)(L)(H2O)(ClO4)](ClO4) (2), (where L=2-amino-1H-benzode]isoquinoline-1,3-(2H)dione (L), phen=1,10-phenanthroline and bpy=2,2 `-bipyridine) have been synthesized and structurally characterized. Structures of the copper complexes 1 and 2 were confirmed by single-crystal X-ray structure determination. The coordination geometry around the copper center of complexes 1 and 2 is distorted octahedral. The plasmid DNA cleavage activity of the complexes has been investigated by agarose gel electrophoresis and the study reveals that both the complexes have high plasmid DNA photo-cleavage activity. The binding interaction ability of the metal complexes with bovine serum albumin (BSA) was investigated using fluorescence spectroscopy. The cytotoxicity of the complexes has been evaluated by MTT (3-4,5-dimethylthiazole-2-yl]-2,5-diphenyltetrazolium bromide) assay against A549 (adenocarcinoma human alveolar basal epithelial cells) and MCF-7 (breast cancer cell line) cell lines in comparison with cis-platin. Complexes 1 and 2 have exhibited better cytotoxic activity than cis-platin against A549 and MCF-7 cell lines. The cellular uptake study and localization of the complexes within the cells have been investigated by fluorescence microscopy. The cell staining and flow cytometry experiments suggest that complexes induce an apoptotic mode of cell death

Study on self-medication among 2nd year medical students

Background: Self-medication is use of medicines by individuals to treat self-recognized symptoms and illness. Self-medication is a common type of self-care behavior in the general public, but medical students differ in such practice, as they have knowledge about drugs and diseases.Methods: The present study involved 100 2nd year final term medical students in “Shivamogga Institute of Medical Sciences,” Shivamogga, Karnataka. Study was questionnaire based, and the results were analyzed by descriptive statistical methods.Results: In our study, 57% were female, and 43% were male. About 60% had knowledge about over the counter (OTC) drugs and considered Ayurveda drugs also OTC drugs. 25% considered self-medication entirely safe, whereas 61% considered self-medication have advantages. Self-medication was preferred by 72% as they felt that there is no need to consult health care professionals for a simple ailment. Self-medication was practiced by 62% students, among which 86% were appropriate, and 48% among them utilized knowledge from previous consultation. In 28% fever was the most common condition and paracetamol was the most commonly used drug.Conclusions: Self-medication was widely practiced among the students. They had good knowledge of OTC drugs. The practice of self-medication was almost appropriate. In general self-medication must be accompanied by appropriate information. Educating benefits and risks of self-medication is very much needed for medical students and the public now a day

A fluoro­phore-labelled copper complex: crystal structure, hybrid cyclic water–perchlorate cluster and biological properties

A fluorophore-labelled copper(II) complex, aquabis(dimethylformamide-O)-(perchlorato-O)[2-(quinolin-2-yl)-1,3-oxazolo[4,5-f][1,10]phenanthroline]cop-per(II) perchlorate monohydrate, [Cu(ClO4)(C22H12N4O)(C3H7NO)2(H2O)]-ClO4H2O, has been synthesized and characterized. A cyclic hydrogen-bondedwater–perchlorate anionic cluster,i.e.[(ClO4)2(H2O)2]2, has been identifiedwithin the structure. Each cyclic anionic cluster unit is interconnected byhydrogen bonding to the cation. The cations join into an infinite hydrogen-bonded chain running in the [010] direction. Furthermore, interaction of thecomplex with calf-thymus DNA (CT-DNA) and cellular localization within thecells was explored. Spectroscopic studies indicate that the compound has a goodaffinity for DNA and stains the nucleus of the cells

The Response of Macro Variables of Emerging and Developed Oil Importers to Oil Price Movements

This paper assesses the impact of crude oil price movements on two macro variables - the gross domestic product (GDP) growth rate and consumer price index inflation rate - in the developed economies of the United States and Japan, and an emerging economy, the People's Republic of China (PRC). These countries were chosen for this research because they are the world's three largest oil consumers. The main objective of this study is to see whether these economies are still reactive to oil price movements. The results obtained suggest that the impact of oil price fluctuations on the GDP growth of the developed oil importers is much lower than on the GDP growth of the emerging economy. The main reasons for this lie in fuel substitution (higher use of nuclear energy, gas, and renewables), a declining population (for Japan), the shale gas revolution (for the United States), and strategic oil stocks and government-mandated energy efficiency targets in developed economies. All of these factors make developed economies more resistant to oil shocks. On the other hand, the impact of oil price movements on the PRC's inflation rate was found to be milder than in the two developed countries that were examined. The main cause for this is that the PRC experiences a larger forward shift in its aggregate supply due to higher growth, which allows it to avoid a massive increase in price levels following oil price shocks

Japan's Lost Decade: Lessons for Other Economies

Japan has suffered from sluggish economic growth and recession since the 1990s, a phenomenon dubbed "Japan's Lost Decade." The People's Republic of China, many countries in the eurozone, and the United States may face similar problems in future and they have been concerned by Japan's long-term recession. This paper will address why Japan's economy has stagnated since the bursting of its economic bubble. Our empirical analysis challenges the beliefs of some western economists, such as Paul Krugman, that the Japanese economy is in a liquidity trap. We argue that Japan's economic stagnation stems from a vertical IS curve rather than a liquidity trap. The impact of fiscal policy has declined drastically, and the Japanese economy faces structural problems rather than a temporary downturn. These structural problems have many causes: an aging demographic (a problem that is frequently overlooked), an over-reliance by local governments on transfers from the central government, and Basel capital requirements that have made Japanese banks reluctant to lend money to startup businesses and small and medium-sized enterprises. This latter issue has discouraged Japanese innovation and technological progress. The paper will address all these issues empirically and theoretically and will provide some remedies for Japan's long-lasting recession

Tamoxifen mechanically deactivates hepatic stellate cells via the G protein-coupled estrogen receptor

Tamoxifen has been used for many years to target estrogen receptor signalling in breast cancer cells. Tamoxifen is also an agonist of the G protein-coupled estrogen receptor (GPER), a GPCR ubiquitously expressed in tissues that mediates the acute response to estrogens. Here we report that tamoxifen promotes mechanical quiescence in hepatic stellate cells (HSCs), stromal fibroblast-like cells whose activation triggers and perpetuates liver fibrosis in hepatocellular carcinomas. This mechanical deactivation is mediated by the GPER/RhoA/myosin axis and induces YAP deactivation. We report that tamoxifen decreases the levels of hypoxia-inducible factor-1 alpha (HIF-1α) and the synthesis of extracellular matrix proteins through a mechanical mechanism that involves actomyosin-dependent contractility and mechanosensing of tissue stiffness. Our results implicate GPER-mediated estrogen signalling in the mechanosensory-driven activation of HSCs and put forward estrogenic signalling as an option for mechanical reprogramming of myofibroblast-like cells in the tumour microenvironment. Tamoxifen, with half a century of safe clinical use, might lead this strategy of drug repositioning.Peer reviewe