Microwave-Assisted Synthesis of Some 1H-1,2,4-Triazol-3-one Derivatives

4-Amino-5-(methyl/ethyl)-2,4-dihydro-3H-1,2,4-triazol-3-one were synthesized from the reaction of (methyl/ethyl)-ester ethoxycarbonyl hydrazone with hydrazine hydrate and then, converted to corresponding Schiff bases using 9H-fluorene- 3-carbaldehyde. Ester, hydrazide and oxadiazole derivatives were synthesized starting from Schiff bases in three steps. All reactions occurred under conventional conditions and microwave irradiation. The obtained results were compared.KEYWORDS Triazole, oxadiazole, hydrazine hydrate, microwave irradiation

Cytotoxic Effect of Turkish Propolis on Liver, Colon, Breast, Cervix and Prostate Cancer Cell Lines

Purpose: To investigate the total polyphenolic and flavonoid contents, antioxidant power and cytotoxic activity of ethanol extracts of Turkish propolis (EEP).Methods: The total polyphenolic and flavonoid contents of EEP were determined by spectrometric methods. Antioxidant power and cytotoxic activity of EEP were evaluated using ferric reducing antioxidant power (FRAP) and MTT assays, respectively.Results: The total polyphenolic and flavonoid contents, and FRAP value of EEP were 124.6 ± 1.5 mg gallic acid/g sample dry weight , 42.0 ± 0.8 mg quercetin/g sample dry weight and 311.0 ± 2.5 mg trolox/g sample dry weight, respectively. EEP exhibited powerful cytotoxic effects against the five human cancer cell lines. The highest cytotoxic activity of Turkish EEP was demonstrated on PC-3 cell line (IC50 = 20.7±3.4 μg/mL).Conclusion: The results demonstrate that EEP is a good source of antioxidant and a natural antitumor agent capable  of reducing cancer cell proliferation.Keywords: Propolis, Polyphenols, Cytotoxic effect, Cancer cell lines, Antioxidant activity Tropical Journal of  Pharmaceutical Research is indexed by Science Citation Index (SciSearch)

Reduction of the Yb valence in YbAl3 nanoparticles

Measurements of specific heat, dc magnetic susceptibility, and Yb LII and LIII x-ray absorption near-edge structure XANES and extended x-ray absorption fine structure EXAFS on YbAl3 milled alloys are reported. X-ray diffraction patterns are consistent with a reduction in particle size down to 10 nm and an increase in the lattice strain up to 0.4% for 120 h of milling time. A decrease in the mean valence from 2.86 for the unmilled alloy to 2.70 for 120 h milled YbAl3 is obtained from the analysis of XANES spectra. From the analysis of spectra in the EXAFS region, an increase in the mean-square disorder of neighbor distance with milling time is detected in good agreement with the results of x-ray diffraction. Size effects strongly influence the magnetic and thermal properties. The value for the maximum of the magnetic susceptibility decreases around 30% for 120 h milled alloy and an excess specific heat, with a peak around 40 K in the milled samples, is derived. These changes in the physical properties along the milled YbAl3 alloys are associated with the reduction in particle size. Such a reduction leads to the existence of a large number of Yb2+ atoms at the surface with respect to the bulk affecting the overall electronic state

Winter Time Concentrations and Size Distribution of Bioaerosols in Different Residential Settings in the UK

The total concentration and size distribution of bioaerosols in three different types of housing (single room in shared accommodation [type I], single bedroom flat in three-storey building [type II] and two- or threebedroom detached houses [type III]) was assessed during the winter. This research was an extension of a previous study carried out in the summer. The measurement campaign was undertaken in winter 2008 and 30 houses were sampled. Samples were taken from kitchens, living rooms, corridors (only in housing type I) and outdoors with an Anderson 6 stage viable impactor. In housing type I, the total geometric mean concentration was highest in the corridor for both bacteria and fungi (3,171 and 1,281 CFU/m3, respectively). In type II residences, both culturable bacteria and fungi were greatest in the living rooms (3,487 and 833 CFU/m3, respectively). The living rooms in type III residences had largest number of culturable bacteria (1,361 CFU/m3) while fungi were highest in kitchens (280 CFU/m3). The concentrations of culturable bacteria and fungi were greater in mouldy houses than non-mouldy houses. A considerable variation was seen in the size distribution of culturable bacteria in type I residences compared to types II and III. For all housing types more than half of culturable bacterial and fungal aerosol were respirable (<4.7 μm) and so have the potential to penetrate into lower respiratory system. Considerable variation in concentration and size distribution within different housing types in the same geographical region highlights the impact of differences in design, construction, use and management of residential built environment on bioaerosols levels and consequent varied risk of population exposure to airborne biological agents. © Springer Science+Business Media B.V. 2012

Differential expression of Lp-PLA2 in obesity and type 2 diabetes and the influence of lipids

Aims/hypothesis Lipoprotein-associated phospholipase A2 (Lp-PLA2) is a circulatory macrophage-derived factor that increases with obesity and leads to a higher risk of cardiovascular disease (CVD). Despite this, its role in adipose tissue and the adipocyte is unknown. Therefore, the aims of this study were to clarify the expression of Lp-PLA2 in relation to different adipose tissue depots and type 2 diabetes, and ascertain whether markers of obesity and type 2 diabetes correlate with circulating Lp-PLA2. A final aim was to evaluate the effect of cholesterol on cellular Lp-PLA2 in an in vitro adipocyte model. Methods Analysis of anthropometric and biochemical variables from a cohort of lean (age 44.4 ± 6.2 years; BMI 22.15 ± 1.8 kg/m2, n = 23), overweight (age 45.4 ± 12.3 years; BMI 26.99 ± 1.5 kg/m2, n = 24), obese (age 49.0 ± 9.1 years; BMI 33.74 ± 3.3 kg/m2, n = 32) and type 2 diabetic women (age 53.0 ± 6.13 years; BMI 35.08 ± 8.6 kg/m2, n = 35), as part of an ethically approved study. Gene and protein expression of PLA2 and its isoforms were assessed in adipose tissue samples, with serum analysis undertaken to assess circulating Lp-PLA2 and its association with cardiometabolic risk markers. A human adipocyte cell model, Chub-S7, was used to address the intracellular change in Lp-PLA2 in adipocytes. Results Lp-PLA2 and calcium-independent PLA2 (iPLA2) isoforms were altered by adiposity, as shown by microarray analysis (p < 0.05). Type 2 diabetes status was also observed to significantly alter gene and protein levels of Lp-PLA2 in abdominal subcutaneous (AbdSc) (p < 0.01), but not omental, adipose tissue. Furthermore, multivariate stepwise regression analysis of circulating Lp-PLA2 and metabolic markers revealed that the greatest predictor of Lp-PLA2 in non-diabetic individuals was LDL-cholesterol (p = 0.004). Additionally, in people with type 2 diabetes, oxidised LDL (oxLDL), triacylglycerols and HDL-cholesterol appeared important predictors, accounting for 59.7% of the variance (p < 0.001). Subsequent in vitro studies determined human adipocytes to be a source of Lp-PLA2, as confirmed by mRNA expression, protein levels and immunochemistry. Further in vitro experiments revealed that treatment with LDL-cholesterol or oxLDL resulted in significant upregulation of Lp-PLA2, while inhibition of Lp-PLA2 reduced oxLDL production by 19.8% (p < 0.05). Conclusions/interpretation Our study suggests adipose tissue and adipocytes are active sources of Lp-PLA2, with differential regulation by fat depot and metabolic state. Moreover, levels of circulating Lp-PLA2 appear to be influenced by unfavourable lipid profiles in type 2 diabetes, which may occur in part through regulation of LDL-cholesterol and oxLDL metabolism in adipocytes

The effect of erythrocyte membranes from diabetic and hypercholesterolemic individuals on human carbonic anhydrase II activity

Erythrocyte membranes regulate many enzyme activities, including carbonic anhydrase II (CA II). Membrane fluidity is associated with alterations in protein function and protein-protein interactions. Objective: The purpose of this study was to show the human CA II (hCA II) activity regulation by human erythrocyte membranes from diabetic and hypercholesterolemic subjects. Materials and methods: Erythrocyte membranes were obtained from diabetic, hypercholesterolemic, and healthy subjects. hCA II activity was measured using the electrometric method. Results: hCA II activity was increased in vitro by membranes from both diabetic and hypercholesterolemic patients, with hypercholesterolemic membranes exhibiting a greater increase. Conclusion: Changes in membrane composition may affect the erythrocyte membranes capacity to increase in vitro hCA II activity. © 2015 Taylor and Francis

Synthesis and antimicrobial activity evaluation of new norfloxacine-azole hybrids

WOS: 000451322900006Norfloxacin-azole hybrids 3 and 6a,b were synthesized starting from norfloxacin. The treatment of these compounds with amines as a one-pot three-component reaction produced the corresponding amino derivatives 4a,b, 7a-g and 8a,b in good yields. The conventional and microwave-assisted methods were used with the latter method being more efficient. The structures of the synthesized compounds were characterized by elemental analysis, IR, H-1 NMR, C-13 NMR and MS. All compounds were screened for their antimicrobial activities. Most of them exhibit excellent antibacterial activity but are not active against selected fungi