Synthesis, spectroscopic characterization and biological applications of Cu(II) and Ni(II) complexes with 2-butyl-4-chloro-5-formylimidazole thiosemicarbazone.

Cu(II) and Ni(II) complexes of 2-butyl-4-chloro-5-formylimidazole thiosemicarbazone (L) are synthesized and characterized by using spectroscopic techniques like elemental analysis, FT-IR, mass spectrometry, electronic and EPR spectra. The complexes are found to have characteristic electronic spectra and the geometry of the complexes are identified as octahedron. Both the complexes are found to exhibit similar anti-microbial activity against the gram –ve and gram +ve bacteria. Anti-cancer activity against the cancer cell lines (MDA-MB 231 cell lines) among the compounds studied for % of viability, the inhibition concentration 50 values were shown by Cu(II)-L complex at 80 mg/ml and by Ni(II)-L complex at 100 mg/ml.

Protection against radiation clastogenecity in mouse bone marrow by Phyllanthus niruri.

The effects of aqueous (PnAq) and alcoholic (PnAl) extract (50-250 mg/kg) of P. niruri on in vivo gamma radiation induced chromosome aberration and in vitro antioxidant activity (50-500 µg/ml) were studied. The antioxidant activity was studied by measuring inhibition of hydroxyl radicals generated by the fenton reaction along with pro-oxidant and iron chelating ability. PnAl showed highly significant in vitro free radical scavenging ability when compared to DMSO above 250 µg/ml concentration. PnAq showed significant pro-oxidant activity while PnAl was devoid of it at the tested concentrations. Exposure to gamma radiation (4 Gy) caused 29.10 % increase in the frequency of chromosomal aberrations. Administration of PnAl (250 mg/kg) showed highly significant decrease in chromosomal aberrations compared to radiation treated group. Radioprotective potential of alcoholic extract was found to be more effective than the aqueous extract. Qualitative phytochemical investigation of PnAq and PnAl revealed the presence of sugars, flavonoids, alkaloid, lignans, polyphenols, tannins, coumarins and saponins. Higher radioprotective effect of the alcoholic extract may be attributed to rich presence of antioxidant polyphenolic compounds.

Docking studies on xanthones of mangosteen as cox-2 inhibitors.

The prostaglandins found in most of the tissues and organs are synthesized by sequential oxidation of cyclooxygenases (COX-1 and COX-2). Prostaglandins synthesized by COX-1 are responsible for the protection of gastrointestinal tract and by COX-2 are responsible for inflammation and pain. The objective of this investigation was to characterize and determine the effect of α-mangostin, β-mangostin and γ-mangostin on COX-1 and COX-2. We have carried out the docking of α, β and γ-mangostin inhibitors into the three dimensional structure of COX-1 and COX-2 enzymes using GOLD software. The inhibitor binding positions and affinity were evaluated using GOLD scoring fitness functions. We identified that amino acid residues Leu52, Arg49, Val33 in COX-1 and Ala18, Ser23, Asp38, Cys22 in COX-2 are important for inhibitor recognition via hydrogen bonding interactions. These hydrogen bonding interactions play an important role for stability of the complex. This information can be exploited to design Mangostin based inhibitors. Our results may be helpful for further experimental investigations.

Metabolic Disturbances in Schizophrenia Patients With Positive, Negative and Cognitive Symptoms.

Elevated cholesterol, triglycerides and glucose are known independent risk factors for coronary heart disease. This study examines the status of cholesterol, triglycerides and glucose of schizophrenia patients with positive, negative and cognitive symptoms and to investigate the association between these levels and obesity. This was a prospective observational study involving samples of patients who met established criteria for schizophrenia and were admitted to the mental health care center, Coimbatore. Glucose, total cholesterol and triglycerides levels increased when schizophrenia patients are treated with anti-psychotic drugs. Although mean changes in glucose and cholesterol levels remained within clinically normal ranges, about one patient in eight studied developed abnormally high glucose, and also one in five patients assessed has abnormal cholesterol levels. The obesity and metabolic disorders observed in the patients were higher than the prevalence in the control group and confirms that there are deregulations of metabolic pathways in schizophrenic patients. The rate of obesity and metabolic disorders observed in this study were higher than the prevalence in the control group sugesting that more attention should be paid to the metabolic condition of psychiatric patients.

Response of S 180 murine tumor to bleomycin in combination with radiation and hyperthermia using micronucleus assay: a multimodality approach for therapeutic augmentation.

Response of a transplantable tumor, S180, grown intradermally in inbred Balb/c mice, was assessed by using micronucleus assay after treating the solid tumors with bleomycin (BLM), radiation (RT) and hyperthermia (HT) vis-a-vis multimodality approach. The frequency of micronuclei (MN) though did not vary greatly during the one week of observation in untreated tumors, it significantly increased in the drug and RT groups at 24 hr post-treatment. However, MN frequency was non-significant in the HT group from the control. A drug dose dependent linear increase in the frequency of MN induction was evident in 10, 15 and 20 mg/kg body weight BLM alone treated groups. Combination of radiation with BLM or HT further increased the MN counts in the bimodality groups. But, MN induction at 24 hr post-treatment in the trimodality group (BLM + RT + HT) was non-significant from that of the bimodality treatments. However, the tumors treated with trimodality treatment presented severe tumor necrosis, indicating increased cell loss, and resulting in immediate tumor regression. In all the bi-modality groups MN counts though declined 3 or 5 days post-treatment, the values remained significantly higher than the control, on day 7 post-treatment. Micronucleus assay could be used as a predictive parameter for the assessment of post-irradiation tumor regression response. However, the tumor response assessment with MN assay alone may not be sufficient and the role of other parameters, such as apoptosis and necrosis, in immediate tumor regression, especially radiosensitive/thermosensitive tumors can not be ignored while taking multimodality approach into consideration for cancer therapy.