Arachidonic acid and calcium metabolism in rnelittin stimulated neutrophils

Melittin, the predominant fraction of bee venom proteins, was studied in an experimental model of human neutrophil granulocytes to reveal its influence on eicosanoid release, metabolism and receptor function in relation to intracellular calcium metabolism. Melittin (2 μmol/l) was as potent as the calcium ionophore A23187 (10 μmol/l) for activation of 5-lipoxygenase, releasing arachidonate only from phosphatidyl-choline and phosphatidyl-ethanolamine of cellular membranes, as judged from the decreases in radioactivity by 15.4% and 30.5%, respectively. The mechanism responsible for the release of arachidonate from cellular membranes is closely coupled to cellular calcium metabolism, and melittin was found to promote calcium entry through receptor gated calcium channels, probably due to an activation of phospholipase A2. Furthermore, a down-regulation of leukotriene B4 receptors was seen. The maximal number of binding sites per cell was reduced from a median of 1520 to 950 with melittin (1 μmol/l). The study has revealed some factors important for the inflammatory mechanisms mediated by melittin

Open Government Data (OGD) Publication as Linked Open Data (LOD): A Survey

Open Government Data (OGD) is a movement that has spread worldwide, enabling the publication of thousands of datasets on the Web, aiming to concretize transparency and citizen participatory governance. This initiative can create value by linking data describing the same phenomenon from different perspectives using the traditional Web and semantic web technologies. A framework of these technologies is linked data movement that guides the publication of data and their interconnection in a machine-readable means enabling automatic interpretation and exploitation. Nevertheless, Open Government Data publication as Linked Open Data (LOD) is not a trivial task due to several obstacles, such as data heterogeneity issues. Many works dealing with this transformation process have been published that need to be investigated thoroughly to deduce the general trends and the issues related to this field. The current work proposes a classification of existing methods dealing with OGD-LOD transformation and a synthesis study to highlight their main trends and challenges

Indium-Mediated Cleavage of the Trityl Group from Protected 1H-Tetrazoles

On treatment with indium metal in MeOH–THF, trityl groups undergo reductive removal from 1H-protected tetrazoles (including aliphatic, aromatic, and heteroaromatic substituents), affording the corresponding free tetrazoles in excellent yields, without any decomposition of the tetrazole ring or reduction of any other group.This work was financially supported by the A.N.D.R.S (Agence Nationale pour le Développement de la Recherche en Santé) (Algérie), the Ministerio de Ciencia e Innovación of Spain (CTQ2011-24165, Consolider Ingenio 2010 CSD2007-00006), The Generalitat Valenciana (PROMETEO/2009/039, PROMETEOII/ 2014/017 and FEDER). We are very grateful to the Spanish Ministerio de Asuntos Exteriores y de Cooperación for a cooperation grant (AP/039112/11)

Zn/MeOH-Mediated Practical and Easy Detritylation of Protected 1-Trityltetrazoles

A practical and low-cost method for the detritylation of 1-titryltetrazoles using zinc and methanol is described. This procedure is versatile and efficient in the deprotection of several protected tetrazoles bearing aliphatic, aromatic, and heteroaromatic substituents, as well as some functional groups, without decomposition of the tetrazole ring.This work was financially supported by the Agence National pour le Développement de la Research en Santé (Algérie) and the Spanish Ministerio de Ciencia e Innovación (CTQ2011-24155, CTQ2011-24165), the Ministerio de Economía y Competitividad (CTQ2013-43446-P, CTQ2014-51912-REDC, CTQ2014-53695-P), FEDER, the Generalitat Valenciana (PROMETEO 2009/039, PROMETEOII/2014/017), and the University of Alicante. We also thank the Spanish Ministerio de Asuntos Exteriores y de Cooperación (AP/039112/11)

Oral Magnesium Supplementation in Chronic Kidney Disease Stages 3 and 4:Efficacy, Safety, and Effect on Serum Calcification Propensity-A Prospective Randomized Double-Blinded Placebo-Controlled Clinical Trial

Chronic kidney disease (CKD) is associated with high cardiovascular morbidity and mortality. Recent evidence suggests that increases in both serum and intracellular magnesium (Mg) can slow or even prevent the development of vascular calcification seen in CKD. Serum calcification propensity (T50) is a novel functional test, which is associated with all-cause mortality in CKD and measures the ability of serum to delay the formation of crystalline nanoparticles. Theoretically, increasing serum Mg should improve T50 and thereby reduce the propensity towards ectopic calcification. Methods: We conducted a randomized placebo-controlled double-blinded clinical trial to investigate the safety of 2 different doses of oral Mg supplementation in subjects with CKD stages 3 and 4 as well as their effects on intracellular Mg and T50. Thirty-six subjects with CKD stages 3 and 4 were randomized to one of 3 groups (placebo, elemental Mg 15 mmol/d or elemental Mg 30 mmol/d) given as slow-release Mg hydroxide and followed for 8 weeks. Results: Thirty-four subjects completed the trial. Intracellular Mg remained stable throughout the trial despite significant increases in both serum and urine Mg. T50 increased significantly by 40 min from 256 ± 60 (mean ± SD) to 296 ± 64 minutes (95% confidence interval, 11–70, P < 0.05) in the Mg 30 mmol/d group after 8 weeks. No serious adverse events related to the study medication were reported during the study. Discussion: Oral Mg supplementation was safe and well tolerated in CKD stages 3 and 4 and improved T50, but did not increase intracellular Mg. Further studies are needed to investigate the long-term effects of Mg supplementation in CKD stage 3 and 4 and whether improvement in calcification propensity is related to clinical endpoints

Effects of Spinal and Peripheral Injection of α1A or α1D Adrenoceptor Antagonists on Bladder Activity in Rat Models with or without Bladder Outlet Obstruction

Purpose Antagonists of α1-adrenergic receptors (α1ARs) relax prostate smooth muscle and relieve voiding and storage symptoms. Recently, increased expression of α1ARs with change of its subtype expression has been proved in bladder outlet obstruction (BOO). To search for the evidence of changes in α1ARs subtype expression and activity in the peripheral and spinal routes, the effects of spinal and peripheral administration of tamsulosin (an α1A/D-selective AR), naftopidil (an α1A/D-selective AR), and doxazosin (non-selective AR) on bladder activity were investigated in a rat model with or without BOO. Methods A total of 65 female Sprague-Dawley rats were divided into the BOO surgery group (n=47) and the sham surgery group (n=18). After 6 weeks, cystometry was assessed before and after intrathecal and intra-arterial administrations of tamsulosin, naftopidil, and doxazosin. Results After intra-arterial administrations of all three drugs, bladder capacity (BC) was increased and maximal intravesical pressure (Pmax) was decreased in both BOO and the sham rat models (P<0.05). After intrathecal administration of all three drugs, BC was increased and Pmax was decreased in only the BOO group. The episodes of involuntary contraction in the BOO rat models were decreased by intra-arterial administration (P=0.031). The increase of BC after intrathercal and intra-arterial administrations of α1ARs was significantly greater in the BOO group than in the sham group (P=0.023, P=0.041). In the BOO group, the increase of BC and decrease in Pmax were greater by intra-arterial administration than by intrathecal administration (P=0.035). There were no significant differences of the degrees of changes in the cystometric parameters among the three different α1ARs. Conclusions Up-regulations of the α1ARs in BOO were observed by the greater increases of BC after α1AR antagonist administrations in the BOO group than in the sham group. However, there were no subtype differences of the α1ARs in functional parameters of bladder activity. In addition, α1ARs also act on the lumbosacral cord which implies that the sensitivity of α1ARs is increased in pathologic models such as BOO. Further evaluation including differential expression of α1ARs in BOO models are need

Les Odonates de l’Oued Isser (Kabylie, Algérie) : statut et déterminants environnementaux de leur distribution

Une étude odonatologique a été réalisée durant six mois successifs, de mai à octobre 2013 à l’Oued Isser, situé dans le nord centre algérien, une région pratiquement inexplorée auparavant. Un total de 19 espèces d’Odonates a été enregistré durant l’échantillonnage mensuel de six stations. Il est à noter la présence de Lestes numidicus et de Platycnemis subdilatata, endémiques du Maghreb. Nos résultats étendent considérablement vers l’ouest la distribution connue de L. numidicus, ayant un statut « données insuffisantes » (DD) sur la liste rouge de l’UICN. À la lumière de la présente étude, on ne propose aucun changement de la classification de la Liste Rouge de l’IUCN à l’exception de L. numidicus qui devrait être classé comme quasi menacé (NT), dans l’attente de nouvelles prospections. Les résultats suggèrent également que la richesse spécifique varierait positivement le long de l’Oued Isser avec la densité de la végétation riveraine. À l’opposé, elle pourrait également être négativement corrélée à la pollution, un facteur important et récurrent de l’érosion de la biodiversité des cours d’eau maghrébins.An odonatological study was carried out during six successive months, from May to October 2013, at Wadi Isser located in the practically unexplored Central North of Algeria. A total of 19 species of Odonata were recorded during the monthly sampling of six stations. Noteworthy was the record of Lestes numidicus and Platycnemis subdilatata, both Maghrebian endemics. Our results extend considerably towards the west the known distribution of L. numidicus, a data deficient (DD) species on the Mediterranean IUCN Red-List. In the light of the present study, no changes in the IUCN Red List classification is proposed with the exception of L. numidicus which should be classified as Near-Threatened (NT), pending further investigations. Results also suggest that the variation of the species richness along Wadi Isser may be related to environmental factors. Species richness was positively associated to the density of the riverine vegetation. In contrast, species richness could also be negatively correlated to pollution, an important and recurrent factor of the erosion of biodiversity of Maghrebian watercourses

Antibodies to infliximab and adalimumab in patients with rheumatoid arthritis in clinical remission:a cross-sectional study

Objective. To investigate if antibodies towards biological TNF-α inhibitors (anti-TNFi Abs) are present in patients with rheumatoid arthritis (RA) in clinical remission and to relate any anti-TNFi Abs to circulating level of TNF-α inhibitor (TNFi). Methods. Patients with RA, treated with infliximab or adalimumab, and in clinical remission (DAS28(CRP) < 2.6) were included from 6 out-patient clinics. In blood samples, presence of anti-TNFi Abs was determined by radioimmunoassay, and concentration of bioactive TNFi was measured by a cell-based reporter gene assay. Results. Anti-TNFi Abs were present in 8/44 patients (18%) treated with infliximab and 1/49 patients (2%) treated with adalimumab (p=0.012). In the former group, anti-TNFi Abs corresponded with low levels of TNFi (p=0.048). Anti-TNFi Ab-positive patients had shorter disease duration at initiation of TNFi therapy (p=0.023) but were similar for the rest of the compared parameters. Conclusions. In RA patients in clinical remission, anti-TNFi Abs occur frequently in patients treated with infliximab, while they occur rarely in patients treated with adalimumab. Presence of anti-infliximab Abs is accompanied by low or undetectable levels of infliximab. These data suggest that continued infliximab treatment may be redundant in a proportion of RA patients treated with infliximab and in clinical remission

Phytochemical characterization, biological screening and corrosion inhibition of mild steel from extracts of Juniperus oxycedrus L.

The aim of this research was to study the effect of solvent polarity and extraction technique of phenolic compounds from Juniperus oxycedrus L. on antioxidant and antibacterial activity. Also, this paper aims to evaluate the anti-corrosive effect of aqueous extracts. In order to evaluate the effect of solvents on the bioactive compound’s extraction efficiency, the samples were prepared with different extraction procedures. The methanolic and ethanolic extracts were prepared by using Soxhlet and maceration extraction and aqueous extracts were obtained by decoction and infusion methods. Moreover, six fractions (petroleum ether, chloroform, ethyl acetate, 1-butanol and aqueous) were prepared by partition of ethanolic extract. All the extracts were subjected to preliminary phytochemical screening; the results show the presence of flavonoids, tannins, alkaloids, triterpenes and steroids. The study of the effect of extraction methods revealed that the decoction is the most suitable for the extraction of phenolic compounds. Moreover, depending on the solvent studied, it was noted that the ethanol showed a high level of flavonoids and the high antioxidant capacity. The extracts were also tested for their antibacterial activity in vitro against two bacterial strains (Escherichia coli and Staphylococcus aureus) using the disc diffusion method. The results of antibacterial showed that the highest activity was attributed to ethanolic extract with a maximum zone of inhibition of 13 mm against Staphylococcus aureus. The corrosion inhibition effect of the aqueous extracts in mild steel in 1 M HCl solution showed that the extracts inhibit effectively corrosion of mild steel