Synthesis of Diarylpyrazoles Containing a Phenylsulphone or Carbonitrile Moiety and their Chalcones as Possible Anti-Inflammatory Agents

A series of chalcone-based diarylpyrazoles containing a phenylsulphone or carbonitrile moiety was synthesized. Thus, 3-acetylpyrazoles 6a–c and 10a–c were used as useful substrates in facile synthesis of functional pyrazoles 7a–f and 11a–f, respectively. The anti-inflammatory activity and ulcerogenic effect were evaluated and some of the obtained products possessed a significant anti-inflammatory activity. 1-[1-(3-Methylphenyl)-5-phenyl-4-(phenylsulfonyl)-1H-pyrazol-3-yl]ethanone (6b) showed a high activity when compared with indomethacin as reference drug with lower gastrointestinal (GI) profile. Furthermore, molecular docking studies were performed in order to rationalize the obtained biological results

Effect of Synthesized Titanium Dioxide Nanofibers Weight Fraction on the Tribological Characteristics of Magnesium Nanocomposites Used in Biomedical Applications

Biomedical applications, such as artificial implants, are very significant for the disabled due to their usage in orthopedics. Nevertheless, available materials in such applications have insufficient mechanical and tribological properties. The current study investigated the mechanical and tribological properties of a biomedical metallic material, magnesium (Mg), after incorporating titanium dioxide nanofibers (TiO2) with different loading fractions. The TiO2 nanofibers were synthesized using the electrospinning technique. The ball-milling technique was utilized to ensure the homogenous distribution of TiO2 nanofibers inside the Mg matrix. Then, samples of the mixed powder with different loading fractions of TiO2 nanofibers, 0, 1, 3, 5, and 10 wt.%, were fabricated using a high-frequency induction heat sintering technique. The physicomechanical and tribological properties of the produced Mg/TiO2 nanocomposites were evaluated experimentally. Results showed an enhancement in mechanical properties and wear resistance accompanied by an increase in the weight fraction of TiO2 nanofibers up to 5%. A finite element model was built to assess the load-carrying capacity of the Mg/TiO2 composite to estimate different contact stresses during the frictional process. The finite element results showed an agreement with the experimental results

Enhance Safety Performance through Quantitative and Qualitative Analysis of Accidents in Egyptian National Railway

Rail transport plays an important role in creating a sustainable future for transport. Safety can be defined as qualitatively or quantitatively to prevent unacceptable risks. Improving safety is the main goal of each railway company as safe operation helps in increasing the level of service offered to the users. This paper deals with quantitative and qualitative analysis of accidents in Egyptian National Railway for annual accidents during the period of 2011 till 2017 for the six zones classified according to causes as absolute values and relative values to determine the worst zones and the most popular causes to improve the safety level and put the corrective plan to minimize the effective of accidents on both economic and safety of the society, to realize this goal a data collections were obtained and traffic fluction were calculated by the use of the official time table in train.km/year for the six zones. The study proposes effective solution for the decision maker to enface this very dangerous problem and improve the economic efficiency of the system, and preserve the environment surrounding the system

Powerful Antioxidant and Pro-Oxidant Properties of Cassia roxburghii DC. Leaves Cultivated in Egypt in Relation to Their Anti-Infectious Activities

Leaf extracts of Cassia roxburghii DC., prepared in petroleum ether, chloroform, ethyl acetate, butanol, and methanol/water (70:30, v/v), were evaluated as antioxidant, pro-oxidant, anti-infectious, and cytotoxic agents. The major metabolite of each extract was identified by chromatographic and spectroscopic means. The redox properties were assessed with a battery of assays, which revealed that the ethyl acetate extract demonstrated an interesting scavenging activity of DPPH and superoxide radicals and an ascorbic acid-like pro-oxidant activity. All the tested extracts showed moderate antiplasmodial activity against a chloroquine-resistant strain of Plasmodium falciparum, by possible disruption of parasite fine redox balance. Cytotoxicity was evaluated against a human breast cancer cell line. The antimicrobial activities of the extracts were estimated against representative bacterial strains (Staphylococcus aureus, Enterococcus hirae, Pseudomonas aeruginosa, Escherichia coli) and fungal species (Candida albicans, Aspergillus niger). The ethylacetate extract possessed the highest redox properties and exhibited the highest antiplasmodial activity; there was no correlation between antibacterial activity and the redox properties of the extracts

Investigation of the Mechanical and Tribological Behavior of Epoxy-Based Hybrid Composite

The main target of this study is to evaluate the impact of hybrid reinforcement using Al2O3 nanoparticles and graphite on the epoxy nanocomposites’ mechanical and tribological properties. Various weight fractions of the reinforcement materials, ranging from 0 to 0.5 wt.%, were incorporated into the epoxy. The aim is to enhance the characteristics and durability of the polymers for potential utilization in different mechanical applications. The addition of hybrid additives consisting of Al2O3 nanoparticles and graphite to the epoxy resin had a noticeable effect on the performance of the epoxy nanocomposites. The incorporation of these additives resulted in increased elasticity, strength, toughness, ductility, and hardness as the concentration of reinforcement increased. The enhancement in the stiffness, mechanical strength, toughness and ductility reached 33.9%, 25.97%, 25.3% and 16.7%, respectively. Furthermore, the frictional tests demonstrated a notable decrease in both the coefficient of friction and wear with the rise of the additives’ weight fraction. This improvement in the structural integrity of the epoxy nanocomposites led to enhanced mechanical properties and wear resistance. The SEM was utilized to assess the surfaces of tested samples and provide insights into the wear mechanism

Metabolomic profile, anti-trypanosomal potential and molecular docking studies of <i>Thunbergia grandifolia</i>

Trypanosomiasis is a protozoan disease transmitted via Trypanosoma brucei. This study aimed to examine the metabolic profile and anti-trypanosomal effect of methanol extract of Thunbergia grandifolia leaves. The liquid chromatography-high resolution electrospray ionisation mass spectrometry (LC-HRESIMS) revealed the identification of fifteen compounds of iridoid, flavonoid, lignan, phenolic acid, and alkaloid classes. The extract displayed a promising inhibitory activity against T. brucei TC 221 with MIC value of 1.90 μg/mL within 72 h. A subsequent in silico analysis of the dereplicated compounds (i.e. inverse docking, molecular dynamic simulation, and absolute binding free energy) suggested both rhodesain and farnesyl diphosphate synthase as probable targets for two compounds among those dereplicated ones in the plant extract (i.e. diphyllin and avacennone B). The absorption, distribution, metabolism, excretion, and toxicity (ADMET) profiling of diphyllin and avacennone were calculated accordingly, where both compounds showed acceptable drug-like properties. This study highlighted the antiparasitic potential of T. grandifolia leaves

Antimicrobial resistance among migrants in Europe: a systematic review and meta-analysis

BACKGROUND: Rates of antimicrobial resistance (AMR) are rising globally and there is concern that increased migration is contributing to the burden of antibiotic resistance in Europe. However, the effect of migration on the burden of AMR in Europe has not yet been comprehensively examined. Therefore, we did a systematic review and meta-analysis to identify and synthesise data for AMR carriage or infection in migrants to Europe to examine differences in patterns of AMR across migrant groups and in different settings. METHODS: For this systematic review and meta-analysis, we searched MEDLINE, Embase, PubMed, and Scopus with no language restrictions from Jan 1, 2000, to Jan 18, 2017, for primary data from observational studies reporting antibacterial resistance in common bacterial pathogens among migrants to 21 European Union-15 and European Economic Area countries. To be eligible for inclusion, studies had to report data on carriage or infection with laboratory-confirmed antibiotic-resistant organisms in migrant populations. We extracted data from eligible studies and assessed quality using piloted, standardised forms. We did not examine drug resistance in tuberculosis and excluded articles solely reporting on this parameter. We also excluded articles in which migrant status was determined by ethnicity, country of birth of participants' parents, or was not defined, and articles in which data were not disaggregated by migrant status. Outcomes were carriage of or infection with antibiotic-resistant organisms. We used random-effects models to calculate the pooled prevalence of each outcome. The study protocol is registered with PROSPERO, number CRD42016043681. FINDINGS: We identified 2274 articles, of which 23 observational studies reporting on antibiotic resistance in 2319 migrants were included. The pooled prevalence of any AMR carriage or AMR infection in migrants was 25·4% (95% CI 19·1-31·8; I2 =98%), including meticillin-resistant Staphylococcus aureus (7·8%, 4·8-10·7; I2 =92%) and antibiotic-resistant Gram-negative bacteria (27·2%, 17·6-36·8; I2 =94%). The pooled prevalence of any AMR carriage or infection was higher in refugees and asylum seekers (33·0%, 18·3-47·6; I2 =98%) than in other migrant groups (6·6%, 1·8-11·3; I2 =92%). The pooled prevalence of antibiotic-resistant organisms was slightly higher in high-migrant community settings (33·1%, 11·1-55·1; I2 =96%) than in migrants in hospitals (24·3%, 16·1-32·6; I2 =98%). We did not find evidence of high rates of transmission of AMR from migrant to host populations. INTERPRETATION: Migrants are exposed to conditions favouring the emergence of drug resistance during transit and in host countries in Europe. Increased antibiotic resistance among refugees and asylum seekers and in high-migrant community settings (such as refugee camps and detention facilities) highlights the need for improved living conditions, access to health care, and initiatives to facilitate detection of and appropriate high-quality treatment for antibiotic-resistant infections during transit and in host countries. Protocols for the prevention and control of infection and for antibiotic surveillance need to be integrated in all aspects of health care, which should be accessible for all migrant groups, and should target determinants of AMR before, during, and after migration. FUNDING: UK National Institute for Health Research Imperial Biomedical Research Centre, Imperial College Healthcare Charity, the Wellcome Trust, and UK National Institute for Health Research Health Protection Research Unit in Healthcare-associated Infections and Antimictobial Resistance at Imperial College London

Predictors of NOAC versus VKA use for stroke prevention in patients with newly diagnosed atrial fibrillation: Results from GARFIELD-AF.

INTRODUCTION: A principal aim of the Global Anticoagulant Registry in the FIELD-Atrial Fibrillation (GARFIELD-AF) was to document changes in treatment practice for patients with newly diagnosed atrial fibrillation during an era when non-vitamin K antagonist oral anticoagulants (NOACs) were becoming more widely adopted. In these analyses, the key factors which determined the choice between NOACs and vitamin K antagonists (VKAs) are explored. METHODS: Logistic least absolute shrinkage and selection operator regression determined predictors of NOAC and VKA use. Data were collected from 24,137 patients who were initiated on AC ± antiplatelet (AP) therapy (NOAC [51.4%] or VKA [48.6%]) between April 2013 and August 2016. RESULTS: The most significant predictors of AC therapy were country, enrolment year, care setting at diagnosis, AF type, concomitant AP, and kidney disease. Patients enrolled in emergency care or in the outpatient setting were more likely to receive a NOAC than those enrolled in hospital (OR 1.16 [95% CI: 1.04-1.30], OR: 1.15 [95% CI: 1.05-1.25], respectively). NOAC prescribing seemed to be favored in lower-risk groups, namely, patients with paroxysmal AF, normotensive patients, and those with moderate alcohol consumption, but also the elderly and patients with acute coronary syndrome. By contrast, VKAs were preferentially used in patients with permanent AF, moderate to severe kidney disease, heart failure, vascular disease, and diabetes and with concomitant AP. CONCLUSION: GARFIELD-AF data highlight marked heterogeneity in stroke prevention strategies globally. Physicians are adopting an individualized approach to stroke prevention where NOACs are favored in patients with a lower stroke risk but also in the elderly and patients with acute coronary syndrome