Development of Novel Thiazolopyrimidines as CDC25B Phosphatase Inhibitors

CDC25 inhibition by thiazolopyrimidines : CDC25 is an attractive target for cancer therapy, as it is overexpressed in numerous cancers and is often associated with tumor aggressiveness and poor prognosis. Based on an in silico/in vitro screen, we developed a series of thiazolopyrimidines to further improve inhibitory activity and cytotoxic properties.

     

Prepartum application of internal teat sealant or intramammary amoxicillin on dairy heifers: Effect on udder health,survival, and performance

Intramammary infusion of antimicrobials (IA) and application of an internal teat sealant (ITS) at the end of the lactation is a common strategy to prevent and treat intramammary infections during the dry period. In heifers, precalving IA has been reported to improve udder health and milk quality; however, the effect of ITS in heifers housed in freestall barns is still unknown. The objective of this study was to investigate the effect of prepartum application of ITS or IA on udder health of dairy heifers. A total of 886 heifers were randomly allocated into 1 of 4 treatment groups when they were 245 ± 3 d pregnant. Control heifers (CON) did not receive any treatment. Heifers in the ITS group received the application of ITS containing 2.6 g of bismuth subnitrate. Animals in the IA group received intramammary administration of 62.5 mg of amoxicillin. Heifers in IA+ITS group received intramammary administration of amoxicillin followed by ITS application. The follow-up period was 270 d in milk (DIM). Clinical mastitis was diagnosed and treated by trained farm personnel throughout the study period. Composite milk somatic cell counts (SCC) were determined monthly for the first 9 mo of lactation by Dairy Herd Improvement Association. Subclinical mastitis was defined as a cow having a SCC >200,000 cells/mL for at least 1 test day and not diagnosed with clinical mastitis during the study period. At 7 ± 3 DIM, composite milk samples were collected for bacteriological analysis for a subset of the study animals. The presence of pathogens in milk at 7 ± 3 DIM was more frequently detected in the CON heifers compared with animals enrolled in the treatment groups. Heifers in IA+ITS group had a decreased incidence of clinical mastitis compared with CON heifers (12.9 vs. 21.4%). Additionally, the incidence of subclinical mastitis was decreased for IA+ITS heifers compared with CON counterparts (20.1 vs. 43.8%). During the first 9 mo of lactation, IA and IA+ITS heifers had lower SCC linear scores compared with ITS and CON counterparts. Although IA+ITS treatment successfully improved udder health, it did not result in better milk yield, fertility, and survivability. In conclusion, ITS alone was not effective in improving udder health; however, the combination of ITS and IA decreased the incidence of clinical and subclinical mastitis during the first 9 mo of lactation. Additionally, IA+ITS had a long-term effect on the SCC linear score throughout the study period.     

Decolourisation of real textile waste using electrochemical techniques: effect of electrode composition

The present paper presents the study of the decolourisation of real textile effluent by constant current electrolysis in a flow-cell using a DSA type material. The effect of using different anode materials (Ti/Ru(0.3)Ti(0.7)O(2); Ti/Ir(0.3)Ti(0.7)O(2); Ti/Ru(X)Sn(1-X)O(2), where X=0.1, 0.2 or 0.3) on the efficiency of colour removal is discussed. Attempts to perform galvanostatic oxidation (40 and 60 mA cm(-2)) on the as-received effluent demonstrate that colour removal and total organic carbon (TOC) removal are limited. In this case the greatest degree of colour removal is achieved when anode containing 90% SnO(2) is used. If the conductivity of the effluent is increased by adding NaCl (0.1 mol L(-1)) appreciable colour/TOC removal is observed. The efficiencies of colour and TOC removal are discussed in terms of the energy per order (E(EO)/kW h m(-3)order(-1)) and energy consumption (E(C)/kW h kg(-1)TOC), respectively. Finally, the extent of colour removal is compared to consent levels presented in the literature.     

Geometrically non-linear approximations on stability and free vibration of composite beams

Second-order formulations based on moderate rotations are often used in finite element models because this approximation facilitates their implementation. However, in some cases this approximation is not enough to obtain all couplings among bending, twisting and stretching deformations for a beam member. Therefore, a simplified second-order formulation may lead to the subsequent loss of some significant terms in the non-linear strains. Without these terms the beam model may predict inaccurate results when the effect of large rotations is important. The present paper investigates the influence of large rotations on the buckling and free vibration behavior of thin-walled composite beam. To carry out this analysis it is necessary to use a geometrically higher-order non-linear beam theory. A distinctive feature of the present study over others available in the literature is that this beam model incorporates, in a full form, the effects of shear flexibility (bending and warping shear). The numerical results show that second-order formulation overestimates the buckling load and natural frequency values when the effect of large rotation is important, and this effect depends on some factors such as load condition and stacking sequences.     

Effect of dietary restriction on the plasma apolipoprotein pattern in cholesterol-fed rabbits

Dietary restriction (half of the control ration) was performed in rabbits given either standard or cholesterol-rich diets. The plasma apolipoproteins were studied on the total, d<1.21, lipoprotein fraction using polyacrylamide gel electrophoresis. A marked rise in the amount of both apo-B and apo-E appeared in cholesterol-fed rabbits and was enhanced by dietary restriction. These results reflect the aggravation of hypercholesterolemia when cholesterol feeding is carried out in underfed rabbits. In all groups only one molecular species of apo-B, identified as apo-B-100, was present after overnight fasting. Thus, lipoproteins which accumulate in the plasma following cholesterol feeding, associated with dietary restriction or not, probably are remnants of hepatogenous triglyceride-rich lipoproteins.     

Synthesis,characterization and magnetic properties of polyaniline-magnetite nanocomposites

In this work we report a new and straightforward method to prepare the polyaniline-magnetite nanocomposite PANI-Fe₃O₄. The method utilizes Fe₃O₄ nanoparticles as the oxidizing agent assisted by UV light to synthesize PANI-Fe₃O₄ magnetic nanocomposite. FTIR and XRD analyses confirm that polyaniline has been obtained in the emeraldine salt form and that the mean diameter of the Fe₃O₄ nanoparticles before synthesis was of the order of 25 nm; for the PANI-Fe₃O₄ nanocomposite in HCl after 4 h of reaction, the mean diameters were of the order of 11 nm. Also, feroxyhite was detected as a secondary phase for the nanocomposite. The dc conductivity results for the pure magnetite were about 2.4 × 10^?6 S cm^?1, while the nanocomposites were of the order of 10^?5 S cm^?1, confirming the increase in conductivity with the increasing amount of PANI. The magnetic measurements showed ferromagnetic behavior for the nanoparticles, with high-saturated magnetization (M_S = 74.30 emu g^?1) and a coercive force of 93.40 Oe. In addition, it was observed that the saturated magnetization for the nanocomposite strongly depends on the reaction time under UV irradiation.     

Fetal Bovine Serum Concentration Affects Δ<Superscript>9</Superscript> Desaturase Activity of <Emphasis Type="Italic">Trypanosoma cruzi</Emphasis>

Fetal bovine serum (FBS) is an important factor in the culture of Trypanosoma cruzi, since this parasite obtains and metabolizes fatty acids (FAs) from the culture medium, and changes in FBS concentration reduce the degree of unsaturation of FAs in phosphoinositides. When T. cruzi epimastigotes were cultured with 5% instead of 10% FBS, and stearic acid was used as the substrate, ∆⁹ desaturase activity decreased by 50%. Apparent K _m and V _m values for stearic acid, determined from Lineaweaver–Burk plots, were 2 μM and 219 pmol/min/mg of protein, respectively. In studies of the requirement for reduced pyridine nucleotide, ∆⁹ desaturase activity reached a maximum with 8 μM NADH and then remained constant; the apparent K _m and V _m were 4.3 μM and 46.8 pmol/min/mg of protein, respectively. The effect of FBS was observed only for ∆⁹ desaturase activity; ∆¹² desaturase activity was not affected. The results suggest that decreased FBS in culture medium is a signal that modulates ∆⁹ desaturase activity in T. cruzi epimastigotes.