Copper complexes as chemical nucleases

Redox active mononuclear and binuclear copper(II) complexes have been prepared and structurally characterized. The complexes have planar N-donor heterocyclic bases like 1,10-phenanthroline (phen), dipyridoquinoxaline (dpq) and dipyridophenazine (dppz) ligands that are suitable for intercalation to B-DNA. Complexes studied for nuclease activity have the formulations [Cu(dpq)2(H2O)] (ClO4)2.H2O (1), [CuL(H2O)2(μ-ox)](ClO4)2 (L = bpy,2; phen,3; dpq,4; and dppz,5) and [Cu(L)(salgly)] (L = bpy,6; phen,7; dpq,8; and dppz,9), where salgly is a tridentate Schiff base obtained from the condensation of glycine and salicylaldehyde. The dpq complexes are efficient DNA binding and cleavage active species. The dppz complexes show good binding ability but poor nuclease activity. The cleavage activity of thebis-dpq complex is significantly higher than thebis-phen complex of copper(II). The nuclease activity is found to be dependent on the intercalating nature of the complex and on the redox potential of the copper(II)/copper(I) couple. The ancillary ligand plays a significant role in binding and cleavage activity

In vitro cytotoxicity of carbon nanoparticles against Hep G 32 cells

The aim of the present study was to evaluate the in vitro toxicity of two multi wall carbon nanotubes (MWCNT) on human hepatocytes (Hep G 32 cell lines). The toxic effects of carbon nanoparticles were analyzed after 48 h of incubation with Hep G 32 cells using MTT assay and also estimated the levels of LDH (that is leakage into the media). The results of the LDH estimation demonstrated that exposure of multi wall carbon nanotubes to hepatocytes (Hep G 32) for 48 h resulted in concentration-dependent increase in LDH leakage and exhibited a significant (p 50 or IC50 values (toxic concentration 50 i.e. concentration of particles inducing 50 %cell mortality) of two nanoparticles were found in the range of 36.99-37.15 μg/ml, which were less than that of quartz (known toxic agent, 39.85 μg/ml), indicating the toxic nature of carbon nanoparticlesColegio de Farmacéuticos de la Provincia de Buenos Aire

Antioxidant, analgesic and anti-inflammatory activities of Leucas cephalotes (Roxb.ex Roth) Spreng

The whole plant of the methanolic extract from Leucas cephalotes was screened for invitro antioxidant (using the DPPH method), invivo analgesic (using hot plate test in mice) and anti-inflammatory (using rat paw edema test) activities. The methanolic extract of Leucas cephalotes (MELC) scavenged the DPPH radicals in a dose-dependent manner. The IC50 value to scavenge DPPH radicals was found to be 421.3µg/ml. A significant (pO extrato metanólico total de Leucas cephalotes foi submetido à triagem para as atividades antioxidante in vitro (utilizando o método DPPH), analgésica (utilizando teste da placa quente, em camundongos) e antiinflamatória (utilizando teste de edema da pata de rato), nas doses de 200 e 400 mg/kg. O extrato metanólico de Leucas cephalotes (MELC) inativou radicais difenil picril hidrazila (DPPH) de forma dose-dependente. O IC50 para essa atividade foi de 421,3 µg/mL. Observou-se atividade analgésica significativa (p<0,0005) a 60 minutos, com 200 mg/kg, e, com 400 mg/kg, observou-se atividade máxima. A resposta antiinflamatória máxima foi produzida, respectivamente, em 3 h e 2 h, com doses de 200 e 400 mg/kg. Estes resultados sugerem que o extrato metanólico de Leucas cephalotes apresenta efeitos analgésico e antiinflamatório significativos, comparáveis aos fármacos padrão

Effect of ABCG2/BCRP Expression on Efflux and Uptake of Gefitinib in NSCLC Cell Lines

BCRP/ABCG2 emerged as an important multidrug resistance protein, because it confers resistance to several classes of cancer chemotherapeutic agents and to a number of novel molecularly-targeted therapeutics such as tyrosine kinase inhibitors. Gefitinib is an orally active, selective EGFR tyrosine kinase inhibitor used in the treatment of patients with advanced non small cell lung cancer (NSCLC) carrying activating EGFR mutations. Membrane transporters may affect the distribution and accumulation of gefitinib in tumour cells; in particular a reduced intracellular level of the drug may result from poor uptake, enhanced efflux or increased metabolism

Role of liver in progression of insulin resistance in relation to IGF-I and insulin levels in rats with acute hepatotoxicity

The aim of the present study was to investigate the role of liver in progression of insulin resistance in relation to IGF-I levels in rats with acute hepatotoxicity, induced by carbon tetrachloride (CCl4) and acetaminophen. Wistar rats were divided into four equal groups of six rats each. Group-I (served as Control1) received olive oil, group-II received CCl4, group-III (served as control 2) received gum acacia and group-IV received acetaminophen. After 48 h of treatment, fasting blood samples were collected to determine biochemical parameters, and liver and pancreas in all groups were collected for histological evaluations. The levels of serum fasting glucose, AST, ALT, ALP, total bilirubin and insulin resistance were Significantly more in group II & IV when compared with their respective control groups. Fasting insulin and IGF-I levels in toxicant treated groups were shown significantly lower than in control groups. The liver sections of toxicant treated rats showed hydropic degeneration (ballooning) in centrilobular hepatocytes with single cell necrosis surrounded by neutrophils. The serum IGF-I level could be a useful marker for identifying subjects at risk of developing type-II diabetes mellitus and possible cardiovascular complications.Colegio de Farmacéuticos de la Provincia de Buenos Aire