Synthesis, biological evaluation and Structure Activity Relationships (SARs) study of 8-(substituted)aryloxycaffeine

AbstractA series of 8-(substituted)aryloxycaffeine were prepared from 8-bromocaffeine and (substituted)phenols by modified Ullmann reaction. In vitro antibacterial activity, inhibitory activity on topoisomerase II and pharmacological activities were evaluated for the synthesized 8-(substituted)aryloxycaffeine. Among the synthesized compounds, 8-(5-chloropyridin-3-yloxy)caffeine (3k) showed strong inhibitory activity (MIC=15.6μg/mL) against the tested gram negative (−) bacteria Salmonella enteritidis. 8-(quinolin-8-yloxy)caffeine (3g) showed the strongest inhibitory activity against topoisomerase II. And the compounds 8-(6-methylpyridin-2-yloxy)caffeine (3j) and 8-(3-chloro-6-(trifluoromethyl)pyridin-2-yloxy)caffeine (3m) showed analgesic effect without the central nervous system stimulation

Evaluation of satellite based indices for gross primary production estimates in a sparse savanna in the Sudan

One of the more frequently applied methods for integrating controls on primary production through satellite data is the Light Use Efficiency (LUE) approach. Satellite indices such as the Normalized Difference Vegetation Index (NDVI), Enhanced Vegetation Index (EVI) and the Shortwave Infrared Water Stress Index (SIWSI) have previously shown promise as predictors of primary production in several different environments. In this study, we evaluate NDVI, EVI and SIWSI derived from the Moderate Resolution Imaging Spectroradiometer (MODIS) satellite sensor against in-situ measurements from central Sudan in order to asses their applicability in LUE-based primary production modeling within a water limited environment. Results show a strong correlation between vegetation indices and gross primary production (GPP), demonstrating the significance of vegetation indices for deriving information on primary production with relatively high accuracy at similar areas. Evaluation of SIWSI however, reveal that the fraction of vegetation apparently is to low for the index to provide accurate information on canopy water content, indicating that the use of SIWSI as a predictor of water stress in satellite data-driven primary production modeling in similar semi-arid ecosystems is limited

Evaluation of the Intestinal Bacterial Community of Local Omani and Cobb 500 Broiler Chickens Raised in an Open-Sided House Using 16S rDNA-Based Analysis

Little is known about how the intestinal bacterial microbiota differs among different strains of chickens raised in an open sided house, predominantly those with lower growth rates, such as Indigenous chickens. Ninety-one-day-old chicks of each strain of chickens were raised in an open-sided house system and fed a conventional corn-soybean meal diet from Day 0–35 days of age. The objective of this study was to assess the relative abundance of bacteria microbiota identified in the intestinal tract of local Omani and Cobb 500 broiler chickens raised in an open-sided house system using 16S rDNA-based analysis. The results obtained showed the diversity of bacterial populations in different intestinal regions of two chicken strains. Bacilli were found in higher numbers and reached 98.8% of the bacteria in the duodenum on Day 5 in Cobb 500 versus 72.5% in the Omani chickens. Local Omani chickens had significantly higher numbers of Clostridia at an early age period. On Day 5 Clostridia comprised 13.1% of the bacteria in the duodenum of local Omani chickens, versus only 0.062% in the Cobb 500. The relative abundance of the bacterial microbiota differed significantly (p <0.05) across different intestinal segments of the two strains of chickens, suggesting that each region generated its bacterial community with different relative abundances

Study protocol: The Dutch 20|30 Postmeningitis study: a cross-sectional follow-up of two historical childhood bacterial meningitis cohorts on long-term outcomes

BACKGROUND: Bacterial meningitis (BM) is a serious, life-threatening infectious disease of the central nervous system that often occurs in young children. The most common severe to moderate sequelae following BM are sensorineural hearing loss, neuromotor disabilities and mental retardation, while subtle sequelae include academic and behavioral disabilities. It is largely unknown whether these more subtle sequelae persist into adolescence and adulthood. Therefore, this study will investigate the very long-term effects of childhood BM in later life. Better understanding of long-term effects and early identification of adverse outcomes after BM are essential for more timely interventions. Additionally, certain single nucleotide polymorphisms (SNPs) are associated with disease severity and might predict adverse sequelae. These include SNPs in genes encoding for pathogen recognition and immune response upon infection. Accordingly, a secondary objective of this study is to investigate the role of genetic variation in BM and use any insights to predict short- and long-term outcomes. METHODS: In the Dutch 20|30 Postmeningitis study, adolescents and young adults (n = 947) from two historical cohorts with a prior episode of BM during childhood will be enrolled into a cross-sectional follow-up investigation using mainly questionnaires that examine executive and behavioral functioning, health-related quality of life, subjective hearing, mood and sleeping disorders, academic performance, and economic self-sufficiency. The results will be compared to normative data by one-sample t-tests. Multivariable regression analysis will be used to assess for any associations with causative pathogens and severity of BM. Participants that complete the questionnaires will be approached to provide a swab for buccal DNA and subsequent sequencing analyses. Logistic regression models will be used to predict sequelae. DISCUSSION: The unique follow-up duration of this cohort will enable us to gain insights into the possible very long-term adverse effects of childhood BM and how these might impact on quality of life. The investigation of host genetic factors will contribute to the development of prediction models which will serve as prognostic tools to identify children who are at high risk of adverse outcome after BM. TRIAL REGISTRATION: Dutch Trial Register NTR-6891. Retrospectively registered 28 December 2017

Assessment of antimalarial activity against Plasmodium falciparum and phytochemical screening of some Yemeni medicinal plants

Developing countries, where malaria is one of the most prevalent diseases, still rely on traditional medicine as a source for the treatment of this disease. In the present study, six selected plants (Acalypha fruticosa, Azadirachta indica, Cissus rotundifolia, Echium rauwalfii, Dendrosicyos socotrana and Boswellia elongata) commonly used in Yemen by traditional healers for the treatment of malaria as well as other diseases, were collected from different localities of Yemen, dried and extracted with methanol and water successfully. The antiplasmodial activity of the extracts was evaluated against fresh clinical isolates of Plasmodium falciparum. The selectivity parameters to evaluate the efficacy of these medicinal plants were measured by in vitro micro test (Mark III) according to World Health Organization (WHO) 1996 & WHO 2001 protocols of antimalarial drug tests. Among the investigated 12 extracts, three were found to have significant antiplasmodial activity with IC50 values less than 4 µg/ml, namely the water extracts of A. fruticosa, A. indica and D. socotrana. Six extracts showed moderate activity with IC50 values ranging from 10 to 30 µg/ml and three appeared to be inactive with IC50 values more than 30 µg/ml. In addition, preliminary phytochemical screening of the methanolic and aqueous extracts indicated the presence of saponins, tannins, flavonoids, terpenoids, polysaccharides and peptides

Enhancement of β-phase in PVDF films embedded with ferromagnetic Gd₅Si₄ nanoparticles for piezoelectric energy harvesting

Self-polarized Gd5Si4-polyvinylidene fluoride (PVDF) nanocomposite films have been synthesized via a facile phase-inversion technique. For the 5 wt% Gd5Si4-PVDF films, the enhancement of the piezoelectric β-phase and crystallinity are confirmed using Fourier transform infrared (FTIR) spectroscopy (phase fraction, Fβ, of 81% as compared to 49% for pristine PVDF) and differential scanning calorimetry (crystallinity, ΔXc, of 58% as compared to 46% for pristine PVDF), respectively. The Gd5Si4 magnetic nanoparticles, prepared using high-energy ball milling were characterized using Dynamic Light Scattering and Vibrating Sample Magnetometry (VSM) to reveal a particle size of ∼470 nm with a high magnetization of 11 emu/g. The VSM analysis of free-standing Gd5Si4-PVDF films revealed that while the pristine PVDF membrane shows weak diamagnetic behavior, the Gd5Si4-PVDF films loaded at 2.5 wt% and 5 wt% Gd5Si4 show enhanced ferromagnetic behavior with paramagnetic contribution from Gd5Si3 phase. The interfacial interactions between Gd5Si4 and PVDF results in the preferential crystallization of the β-phase as confirmed via the shift in the CH2 asymmetric and symmetric stretching vibrations in the FTIR. These results confirm the magnetic Gd5Si4 nanoparticles embedded in the PVDF membrane lead to an increased β-phase fraction, which paves the way for future efficient energy harvesting applications using a combination of magnetic and piezoelectric effects

Performance evaluation of secured versus non-secured EIGRP routing protocol

Routing is the process of forwarding data across an inter-network from a designated source to a final destination.Along the way from source to destination, at least one intermediate node is considered. Due to the major role that routing protocols play in computer network infrastructures, special cares have been given to routing protocols with built-in security constraints.In this paper, we evaluate the performance of EIGRP routing protocol in the case of secured and non-secured routing traffic.This is done through studying and analyzing EIGRP routing traffic with and without security rules.A network model of four Cisco routers, from both software and hardware perspectives, has been employed and a traffic generation and analysis tools have been developed and used to generate traffic data and to measure the delay for performance evaluation.The results show that the average delay in the secured case can become significantly larger than the unsecured case even in steady state conditions.The differences between the delays are exponential and reach a steady state towards the end of the experiment

Box–Behnken Response Surface Design of Polysaccharide Extraction from Rhododendron arboreum and the Evaluation of Its Antioxidant Potential

© 2020 by the authors. In the present investigation, the ultrasound-assisted extraction (UAE) conditions and optimization of Rhododendron arboreum polysaccharide (RAP) yield were studied by a Box–Behnken response surface design and the evaluation of its antioxidant potential. Three parameters that affect the productivity of UAE, such as extraction temperature (50–90 ◦C), extraction time (10–30 min), and solid–liquid ratio (1–2 g/mL), were examined to optimize the yield of the polysaccharide percentage. The chromatographic analysis revealed that the composition of monosaccharides was found to be glucose, galactose, mannose, arabinose, and fucose. The data were fitted to polynomial response models, applying multiple regression analysis with a high coefficient of determination value (R2 = 0.999). The data exhibited that the extraction parameters have significant effects on the extraction yield of polysaccharide percentage. Derringer’s desirability prediction tool was attained under the optimal extraction conditions (extraction temperature 66.75 ◦C, extraction time 19.72 min, and liquid–solid ratio 1.66 mL/g) with a desirability value of 1 yielded the highest polysaccharide percentage (11.56%), which was confirmed through validation experiments. An average of 11.09 ± 1.65% of polysaccharide yield was obtained in optimized extraction conditions with a 95.43% validity. The in vitro antioxidant effect of polysaccharides of R. arboreum was studied. The results showed that the RAP extract exhibited a strong potential against free radical damage

Controlling the Oxidation of Magnetic and Electrically Conductive Solid-Solution Iron-Rhodium Nanoparticles Synthesized by Laser Ablation in Liquids

This study focuses on the synthesis of FeRh nanoparticles via pulsed laser ablation in liquid and on controlling the oxidation of the synthesized nanoparticles. Formation of monomodal γ-FeRh nanoparticles was confirmed by transmission electron microscopy (TEM) and their composition confirmed by atom probe tomography (APT). For these particles, three major contributors to oxidation were analysed: (1) dissolved oxygen in the organic solvents, (2) the bound oxygen in the solvent and (3) oxygen in the atmosphere above the solvent. The decrease of oxidation for optimized ablation conditions was confirmed through energy-dispersive X-ray (EDX) and Mössbauer spectroscopy. Furthermore, the time dependence of oxidation was monitored for dried FeRh nanoparticles powders using ferromagnetic resonance spectroscopy (FMR). By magnetophoretic separation, B2-FeRh nanoparticles could be extracted from the solution and characteristic differences of nanostrand formation between γ-FeRh and B2-FeRh nanoparticles were observed