13 research outputs found

    Second Generation Steroidal 4-Aminoquinolines Are Potent, Dual-Target Inhibitors of the Botulinum Neurotoxin Serotype A Metalloprotease and P. falciparum Malaria

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    Significantly more potent second generation 4-amino-7-chloroquinoline (4,7-ACQ) based inhibitors of the botulinum neurotoxin serotype A (BoNT/A) light chain were synthesized. Introducing an amino group at the C(3) position of the cholate component markedly increased potency (IC50 values for such derivatives ranged from 0.81 to 2.27 mu M). Two additional subclasses were prepared: bis(steroidal)-4,7-ACQ derivatives and bis(4,7-ACQ)cholate derivatives; both classes provided inhibitors with nanomolar-range potencies (e.g., the K-i of compound 67 is 0.10 mu M). During BoNT/A challenge using primary neurons, select derivatives protected SNAP-25 by up to 89%. Docking simulations were performed to rationalize the compounds' in vitro potencies. In addition to specific residue contacts, coordination of the enzyme's catalytic zinc and expulsion of the enzyme's catalytic water were a consistent theme. With respect to antimalarial activity, the compounds provided better IC90 activities against chloroquine resistant (CQR) malaria than CQ, and seven compounds were more active than mefloquine against CQR strain W2

    Alumina/silica supported K2CO3 as a catalyst for biodiesel synthesis from sunflower oil

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    The new type of catalyst for fatty acid methyl esters (FAME or biodiesel) synthesis with K2CO3 as active component on alumina/silica support was synthesized using sol-gel method. Corresponding catalyst (xerogel) was prepared by 12 h drying the wet gel in air at 300 °C, 600 °C or 1000 °C at atmospheric pressure. The catalysts activity in the methanolysis of sunflower oil was compared to the activity of the pure K2CO3. The effects of various reaction variables on the yield of FAME were investigated. It was found that the temperature of 120 °C and methanol to oil molar ratio of 15:1, are optimal conditions for FAME synthesis with synthesized catalyst. Repeated use of same amount of catalyst indicated that effect of potassium leaching obviously existed leading to decrease of catalyst activity

    Application of hybrid boundary element method: Example of semishperical ground inhomogeneity

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    One new, so-called hybrid boundary element method (HBEM) is presented in this paper. It is a recently proposed numerical method for stationary and quasi-stationary EM field analysis. The method application is illustrated on the example of solving the problem of modelling hemispherical ground inhomogeneity influence on grounding system. The applied procedure also includes using of quasi-stationary image-theory. The obtained results are compared with those ones based on using the Green’s function for the point source inside semi-spherical inhomogeneities as well as with the results obtained by applying COMSOL program package. [TR 33008

    Application of Hybrid Boundary Element Method on Modelling of Hemispherical Ground Inhomogeneity

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    The procedure for modelling ground inhomogeneity influence on grounding system based on socalled hybrid boundary element method (HBEM) is given in this paper. The HBEM is a recently proposed numerical method for stationary or quasi-stationary EM field analysis. The obtained results are compared with those based on using the Green’s function for the point source inside a semispherical inhomogeneity

    Modelling and Simulation of Electromagnetic Radiation Effects of Mobile Phones on Teeth with an Amalgam Filling

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    Excessive everyday use of mobile phones and wireless communication systems has produced life in electromagnetic fields and growing public concern about possible effects on human health. All these devices operate close to the head and body and electromagnetic waves leave part of their energy in the matter through which they pass. There has been a lot of research on the toxic effects of amalgam fillings that are believed to be the main source of human total mercury body burden but there is not sufficient knowledge about the influence of electromagnetic radiation from mobile phone on amalgam filling and how that affects human health. Electrical engineering has the task to produce devices that improve the quality of human life without any negative effects, and to ensure the safety of new products and technologies. Using electromagnetic simulation to obtain electromagnetic quantities in the head and teeth and linking these results to physical and physical-chemical processes in the matter has led to advances in clarifying these issues. In general, the conclusion is that the use of mobile phones can lead to increased absorption of energy and other electromagnetic quantities in teeth and filling of teeth and cause increased release of mercury and toxicological effects to health associated with the intake of mercury in the human organism

    Metabolic changes in Euphorbia palusrtis latex after fungal infection

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    The variations of metabolic profile of the latex of wild-growing Euphorbia palustris was carried out using multivariate analysis of NMR spectral data. One population was infected with fungi Fusarium sporotrichioides, Fusarium proliferatum and Alternaria alternata, while the other consisted of healthy plant species. The non-polar metabolites of latex extracts such as benzoyl ingenol-laurate, amyrin decadienoate esters, cis-1,4-polyisoprene, and 24-methylenecycloartanol were identified using H-1 and 2D NMR spectra. Principal component analysis of H-1 NMR data provided a clear discrimination between the latex of infected and healthy plants. Minimum inhibitory concentration and minimum fungicidal concentration values of the latex extracts of healthy and infected plants were determined. The latex of infected plants was found to contain higher levels of benzoyl ingenol-laurate and 24-methylenecycloartanol, of which concentrations were strongly correlated with the antifungal activities of the latex. (C) 2016 Elsevier Ltd. All rights reserved.Supplementary material: [http://cherry.chem.bg.ac.rs/handle/123456789/3564

    Sorbus aucuparia and Sorbus aria as a Source of Antioxidant Phenolics, Tocopherols, and Pigments.

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    Due to its nutritive and medicinal properties, berries of some Sorbus species are used for the preparation of jams and jelly as well as in traditional medicine. On the other hand, their chemical composition is not much studied especially of those grown in Balkan Peninsula. We have analyzed individual phenolics, tocopherols, carotenoids and chlorophylls using HPLC in berries from Sorbus aucuparia and Sorbus aria collected in different localities in Serbia and Montenegro together with the amounts of total phenolics and proanthocyanidins as well as their radical scavenging activity against DPPH radical. Berries of S. aucuparia were richer source of polyphenolics in comparision with S. aria and, regardless the species and locality, caffeoylquinic acids such as neochlorogenic and chlorogenic acid were the most abundant compounds. Among analyzed tocopherols the most abundant in all samples was α-tocopherol (0.48 - 19.85 μg/g dw) as it was β-carotene among carotenoids (mean concentration of 0.98 μg/g dw in S. aucuparia and 0.40 μg/g dw in S. aria, respectively). Correlation between total phenolics and DPPH radical scavenging activity was noticed. Our study represents comprehensive report on chemical composition of S. aucuparia and S. aria which could contribute to a better understanding of their quality.Chemistry & Biodiversity, 2017, 14, 12, e170032
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