Search results for: active compounds
5141 Inhibition of 3-Deoxy-D-Arabino-Heptulosonate 7-Phosphate Synthase from Mycobacterium Tuberculosis Using High Throughput Virtual Screening and Molecular Dynamics Studies
Authors: Christy Rosaline, Rathankar Roa, Waheeta Hopper
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Persistence of tuberculosis, emergence of multidrug-resistance and extensively drug-resistant forms of the disease, has increased the interest in developing new antitubercular drugs. Developing inhibitors for 3-deoxy-D-arabino-heptulosonate 7-phosphate synthase from Mycobacterium tuberculosis (MtbDAH7Ps), an enzyme involved in shikimate pathway, gives a selective target for antitubercular agents. MtbDAH7Ps was screened against ZINC database, and shortlisted compounds were subjected to induce fit docking. Prime/Molecular Mechanics Generalized Born Surface Area calculation was used to validate the binding energy of ligand-protein complex. Molecular Dynamics analysis for of the lead compounds–MtbDAH7Ps complexes showed that the backbone of MtbDAH7Ps in their complexes were stable. These results suggest that the shortlisted lead compounds ZINC04097114, ZINC15163225, ZINC16857013, ZINC06275603, and ZINC05331260 could be developed into novel drug leads to inhibit DAH7Ps in Mycobacterium tuberculosis.Keywords: MtbDAH7Ps, Mycobacterium tuberculosis, HTVS, molecular dynamics
Procedia PDF Downloads 1795140 Microseismicity of the Tehran Region Based on Three Seismic Networks
Authors: Jamileh Vasheghani Farahani
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The main purpose of this research is to show the current active faults and active tectonic of the area by three seismic networks in Tehran region: 1-Tehran Disaster Mitigation and Management Organization (TDMMO), 2-Broadband Iranian National Seismic Network Center (BIN), 3-Iranian Seismological Center (IRSC). In this study, we analyzed microearthquakes happened in Tehran city and its surroundings using the Tehran networks from 1996 to 2015. We found some active faults and trends in the region. There is a 200-year history of historical earthquakes in Tehran. Historical and instrumental seismicity show that the east of Tehran is more active than the west. The Mosha fault in the North of Tehran is one of the active faults of the central Alborz. Moreover, other major faults in the region are Kahrizak, Eyvanakey, Parchin and North Tehran faults. An important seismicity region is an intersection of the Mosha and North Tehran fault systems (Kalan village in Lavasan). This region shows a cluster of microearthquakes. According to the historical and microseismic events analyzed in this research, there is a seismic gap in SE of Tehran. The empirical relationship is used to assess the Mmax based on the rupture length. There is a probability of occurrence of a strong motion of 7.0 to 7.5 magnitudes in the region (based on the assessed capability of the major faults such as Parchin and Eyvanekey faults and historical earthquakes).Keywords: Iran, major faults, microseismicity, Tehran
Procedia PDF Downloads 3685139 Distribution of Phospholipids, Cholesterol and Carotenoids in Two-Solvent System during Egg Yolk Oil Solvent Extraction
Authors: Aleksandrs Kovalcuks, Mara Duma
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Egg yolk oil is a concentrated source of egg bioactive compounds, such as fat-soluble vitamins, phospholipids, cholesterol, carotenoids and others. To extract lipids and other fat-soluble nutrients from liquid egg yolk, a two-step extraction process involving polar (ethanol) and non-polar (hexane) solvents were used. This extraction technique was based on egg yolk bioactive compounds polarities, where non-polar compound was extracted into non-polar hexane, but polar in to polar alcohol/water phase. But many egg yolk bioactive compounds are not strongly polar or non-polar. Egg yolk phospholipids, cholesterol and pigments are amphipatic (have both polar and non-polar regions) and their behavior in ethanol/hexane solvent system is not clear. The aim of this study was to clarify the behavior of phospholipids, cholesterol and carotenoids during extraction of egg yolk oil with ethanol and hexane and determine the loss of these compounds in egg yolk oil. Egg yolks and egg yolk oil were analyzed for phospholipids (phosphatidylcholine (PC) and phosphatidylethanolamine (PE)), cholesterol and carotenoids (lutein, zeaxanthin, canthaxanthin and β-carotene) content using GC-FID and HPLC methods. PC and PE are polar lipids and were extracted into polar ethanol phase. Concentration of PC in ethanol was 97.89% and PE 99.81% from total egg yolk phospholipids. Due to cholesterol’s partial extraction into ethanol, cholesterol content in egg yolk oil was reduced in comparison to its total content presented in egg yolk lipids. The highest amount of lutein and zeaxanthin was concentrated in ethanol extract. The opposite situation was observed with canthaxanthin and β-carotene, which became the main pigments of egg yolk oil.Keywords: cholesterol, egg yolk oil, lutein, phospholipids, solvent extraction
Procedia PDF Downloads 5095138 Linear Semi Active Controller of Magneto-Rheological Damper for Seismic Vibration Attenuation
Authors: Zizouni Khaled, Fali Leyla, Sadek Younes, Bousserhane Ismail Khalil
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In structural vibration caused principally by an earthquake excitation, the most vibration’s attenuation system used recently is the semi active control with a Magneto Rheological Damper device. This control was a subject of many researches and works in the last years. The big challenges of searchers in this case is to propose an adequate controller with a robust algorithm of current or tension adjustment. In this present paper, a linear controller is proposed to control the MR damper using to reduce a vibrations of three story structure exposed to El Centro’s 1940 and Boumerdès 2003 earthquakes. In this example, the MR damper is installed in the first floor of the structure. The numerical simulations results of the proposed linear control with a feedback law based on clipped optimal algorithm showed the feasibility of the semi active control to protecting civil structures. The comparison of the controlled structure and uncontrolled structures responses illustrate clearly the performance and the effectiveness of the simple proposed approach.Keywords: MR damper, seismic vibration, semi-active control
Procedia PDF Downloads 2855137 The Collagen and Glycosaminoglycnas Isolated from Salmo Salar Skin
Authors: Beata Kaczmarek-Szczepańska, Lidia Zasada
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Marine collagens such as fish skin, bone, cartilage, and scales, including both marine vertebrates and invertebrates sources, are more bioavailable compared to bovine or porcine collagen and have a higher absorption capability and more rapid bloodstream circulation due to their low molecular weight and small particle size. Fish skin may be used as a source of bioactive compounds. The advantage is that fish skin is a by-product of the food industry. The subject of the study is a lyophilizate consisting of a mixture of compounds from the group of glycosaminoglycans and collagen obtained as a result of processing fish skins. Bioactive compounds may find biomedical use in the production of dressing materials for wounds or in tissue engineering for the production of scaffolds for cells. Collagen and glycosaminoglycans were isolated from Salmo salar skin. The final mixture was obtained by the freeze-drying method. In the obtained lyophilizate, the content of amino acids was studied as well as the presence of polysaccharides. The studies showed the presence of glycine, proline, and hydroxyproline, which are the main amino acids of collagen. The HPLC analysis showed the presence of glucose which is a product of polysaccharides hydrolyzation and then reduction of glucuronic acid. It may be assumed that the lyophilizate contains both collagen and polysaccharide, which is probably hyaluronic acid. Acknowledgment: This work was carried out as a result of research project no. TANGO-V-A/0020/2021 financed by the National Centre for Research and Development.Keywords: collagen, glycosaminoglycans, bioactive compounds, fish skin
Procedia PDF Downloads 1165136 Dehalogenation of Aromatic Compounds in Wastewater by Bacterial Cultures
Authors: Anne Elain, Magali Le Fellic
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Halogenated Aromatic Compounds (HAC) are major organic pollutants that are detected in several environmental compartments as a result of their widespread use as solvents, pesticides and other industrial chemicals. The degradation of HAC simultaneously at low temperature and under saline conditions would be useful for remediation of polluted sites. Hence, microbial processes based on the metabolic activities of anaerobic bacteria are especially attractive from an economic and environmental point of view. Metabolites are generally less toxic, less likely to bioaccumulate and more susceptible for further degradation. Studies on biological reductive dehalogenation have largely been restricted to chlorinated compounds while relatively few have focussed on other HAC i.e., fluorinated, brominated or iodinated compounds. The objectives of the present work were to investigate the biodegradation of a mixture of triiodoaromatic molecules in industrial wastewater by an enriched bacterial consortium. Biodegradation of the mixture was studied during batch experiments in an anaerobic reactor. The degree of mineralization and recovery of halogen were monitored by HPLC-UV, TOC analysis and potentiometric titration. Providing ethanol as an electron donor was found to stimulate anaerobic reductive dehalogenation of HAC with a deiodination rate up to 12.4 mg.L-1 per day. Sodium chloride even at high concentration (10 mM) was found to have no influence on the degradation rates nor on the microbial viability. An analysis of the 16S rDNA (MicroSeq®) revealed that at least 6 bacteria were predominant in the enrichment, including Pseudomonas aeruginosa, Pseudomonas monteilii, Kocuria rhizophila, Ochrobacterium anthropi, Ralstonia pickettii and Rhizobium rhizogenes.Keywords: halogenated aromatics, anaerobic biodegradation, deiodination, bacterial consortium
Procedia PDF Downloads 1775135 Representativity Based Wasserstein Active Regression
Authors: Benjamin Bobbia, Matthias Picard
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In recent years active learning methodologies based on the representativity of the data seems more promising to limit overfitting. The presented query methodology for regression using the Wasserstein distance measuring the representativity of our labelled dataset compared to the global distribution. In this work a crucial use of GroupSort Neural Networks is made therewith to draw a double advantage. The Wasserstein distance can be exactly expressed in terms of such neural networks. Moreover, one can provide explicit bounds for their size and depth together with rates of convergence. However, heterogeneity of the dataset is also considered by weighting the Wasserstein distance with the error of approximation at the previous step of active learning. Such an approach leads to a reduction of overfitting and high prediction performance after few steps of query. After having detailed the methodology and algorithm, an empirical study is presented in order to investigate the range of our hyperparameters. The performances of this method are compared, in terms of numbers of query needed, with other classical and recent query methods on several UCI datasets.Keywords: active learning, Lipschitz regularization, neural networks, optimal transport, regression
Procedia PDF Downloads 815134 The Cytoprotective Role of Antioxidants in Mammalian Cells Exposed to Variable Temperature, Pressure Overload and Radiation in the Stratosphere
Authors: Dawid Przystupski, Agata Gorska, Paulina Rozborska, Weronika Bartosik, Olga Michel, Joanna Rossowska, Anna Szewczyk, Malgorzata Drag-Zalesinska, Jedrzej Gorski, Julita Kulbacka
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Researchers are still looking for an answer to the question which has been fascinating the mankind for generations, specifically – is there life beyond Earth? As long as routine flights to other planets remain beyond our reach, there is a need to find alternative ways to conduct the astrobiological research. It is worth noticing that the part of the Earth’s atmosphere, stratosphere, has been found to show subcosmic environmental conditions, namely temperatures around -50°C, very rarefied air, increased cosmic radiation and the Sun’s ultraviolet radiation. This phenomenon gives rise to the opportunity for the use of stratospheric environment as a research model for the space conditions. Therefore the idea of conducting astrobiological experiments during the stratospheric flights arose. Up to now, the preliminary work in this field included launching balloons containing solely microbiological samples into the stratosphere to figure out if they would be able to survive under the stratospheric conditions. In our study, we take this concept further, sending the human healthy and cancerous cells treated with various compounds to investigate whether these medicines are capable to protect the cells against stratospheric stress. Due to oxidative stress caused by ionizing radiation and temperature shock, we used natural compounds which display antioxidant properties. In this way, we were able to reduce the reactive oxygen species production affecting cells, which results in their death. After-flight laboratory tests of biological samples from the stratosphere have been performed and indicated the most active antioxidants as potential agents which can minimize the harmful impacts of stratospheric conditions, especially radiation and temperature.Keywords: antioxidants, stratosphere, balloon flight, oxidative stress, cell death, radiation
Procedia PDF Downloads 1385133 Active Noise Cancellation in the Rectangular Enclosure Systems
Authors: D. Shakirah Shukor, A. Aminudin, Hashim U. A., Waziralilah N. Fathiah, T. Vikneshvaran
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The interior noise control is essential to be explored due to the interior acoustic analysis is significant in the systems such as automobiles, aircraft, air-handling system and diesel engine exhausts system. In this research, experimental work was undertaken for canceling an active noise in the rectangular enclosure. The rectangular enclosure was fabricated with multiple speakers and microphones inside the enclosure. A software program using digital signal processing is implemented to evaluate the proposed method. Experimental work was conducted to obtain the acoustic behavior and characteristics of the rectangular enclosure and noise cancellation based on active noise control in low-frequency range. Noise is generated by using multispeaker inside the enclosure and microphones are used for noise measurements. The technique for noise cancellation relies on the principle of destructive interference between two sound fields in the rectangular enclosure. One field is generated by the original or primary sound source, the other by a secondary sound source set up to interfere with, and cancel, that unwanted primary sound. At the end of this research, the result of output noise before and after cancellation are presented and discussed. On the basis of the findings presented in this research, an active noise cancellation in the rectangular enclosure is worth exploring in order to improve the noise control technologies.Keywords: active noise control, digital signal processing, noise cancellation, rectangular enclosure
Procedia PDF Downloads 2725132 In vivo Genotoxicity Testing of Sesbania Grandiflora (Katuray) Flower Methanolic Extract
Authors: Levylee Bautista, Dawn Grace Santos, Aishwarya Veluchamy, Jesusa Santos, Ghafoor, Jr. I Haque, Rodolfo Rafael
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The booming interest in using natural compounds as an alternative to conventional medications has paved way to focus the attention on plants that provide rich sources of bioactive phytochemicals. For regulatory purposes, evaluation of the genotoxic effects of such alternatives is therefore empirical as part of the plant’s hazard assessment. Sesbania grandiflora is among the plants used as a traditional remedy in folk medicine and a subject of research for its medicinal benefits. This study aimed to evaluate the genotoxic potential induced by S. grandiflora flower methanol extract (SGFME) in terms of the frequency of micronucleus (MN) in polychromatic erythrocyte (PCE) (MNPCE) and PCE ratio employing the micronucleus assay. The frequency of MN was examined in bone marrow cells (BMCs) obtained from male Swiss albino mice exposed in vivo to four different concentrations (11.25, 22.5, 40, and 90 mg/kg) of SGFME and MMC (70 mg/kg; positive control) and sacrificed 24 hours post-intraperitoneal injection. Results showed a significant (p < 0.01) rate of MNPCEs for 11.25 and 22.5 tested concentrations of SGFME and is comparable with the MMC-treated mice. Although PCE ratio values in all doses of SGFME-treated mice were over 0.20, it is worth noting that 40 and 90 tested concentrations of SGFME-treated mice exhibited the lowest value, i.e., 0.22 and 0.28, respectively. The present study has demonstrated that S. grandiflora possesses genotoxic potential for murine BMCs. Such activity could be ascribed from the bioactive compounds present in S. grandiflora that require further isolation and characterization of the active molecules. Likewise, findings of this study warrant a caution of the use of S. grandiflora insomuch as further investigations do not demonstrate their safety.Keywords: genotoxicity, micronucleus, phytochemicals, Sesbania grandiflora
Procedia PDF Downloads 1435131 Synthesis of Novel Metallosurfactants for Drug Delivery
Authors: Fatima Zohra Belghait, Nawal Cheikh, Oscar Palacios, Ramon Barnadas, Pau Bayon
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Metalloporphyrin and its derivatives play an important role in different scientific areas due to its tetradentate vacant site in the center that is suitable for metal coordination. Metalosomes (MTS) are supramolecular aggregates (similar to liposomes) generated by the self-assembly of compounds similar to phospholipids (with a polar and a hydrophobic part), but incorporating, as part of their membrane, molecules that contain bound metals. The aim of our work is to synthesise metalosomes containing catioinc amphiphilic porphyrin and their complexes with Fe and Cu to study their therapeutical applications. All synthesized compounds were confirmed with Dynamic Light Scattering; elemental analysis, Ultraviolet–visible spectroscopyKeywords: metalloporphyrin, amphiphilique porphyrin, metalosomes, supramolecular
Procedia PDF Downloads 85130 Ionic Liquid 1-Butyl-3-Methylimidazolium Bromide as Reaction Medium for the Synthesis of Flavanones under Solvent-Free Conditions
Authors: Cecilia Espindola, Juan Carlos Palacios
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Flavonoids are a large group of natural compounds which are found in many fruits and vegetables. A subgroup of these called flavanones display a wide range of biological activities, and they also have an important physiological role in plants. The ionic liquid (ILs) are compounds consisting of an organic cation with an organic or inorganic anion. Due to its unique properties such as high electrical conductivity, wide temperature range of the liquid state, thermal and electrochemical stability, high ionic density and low volatility and flammability, are considered as ecological solvents in organic synthesis, catalysis, electrolytes in accumulators, and electrochemistry, non-volatile plasticizers, and chemical separation. It was synthesized ionic liquid IL 1-butyl-3-methylimidazolium bromide free-solvent and used as reaction medium for flavanones synthesis, under several reaction conditions of temperature, time and production. The obtained compounds were analyzed by melting point, elemental analysis, IR and UV-vis spectroscopy.Keywords: 1-butyl-3-methylimidazolium bromide, flavonoids, free-solvent, IR spectroscopy
Procedia PDF Downloads 1205129 Gender Agreement in Italian Compounds with Capo-
Authors: Irene Lami, Silvia Micheli, Jan Radimský, Joost van de Weijer
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The present study examines gender agreement in Italian compounds with "capo-". Compounds containing "capo-" as the first element is highly productive in Italian and are attested from the earliest stages of the language, with "capo" indicating a prominent role in a group. This type of compound has become progressively more productive over time, establishing itself in the language to indicate human referents with a leadership role over someone or something belonging to both subordinate and coordinate compound categories. In light of the debates on the use of inclusive language, especially with regard to female professional titles in Italian, the gender agreement of the word "capo" is investigated, which in addition to social resistance, also encounters etymological resistance. Regarding the gender agreement of the word "capo-" as the first element of compounds, in addition to social and etymological resistances, morphological constraints must also be considered. In our experiment, 190 native informants were asked to match the gender of the given the word in a sentence, thinking of female referents. The results confirm a scalar hypothesis of gender agreement (i.e., titles traditionally attributed to women > titles traditionally attributed to men > the word "capo" in isolation > the word "capo-" as an element of subordinate compound > the word “capo-“ as an element of a coordinate compound). A significant interplay with number marking is also shown, as words are inflected in gender when the trait +plural is present. Moreover, the results show that, contrary to what is prescriptively established, speakers do inflect the word "capo" according to gender, in limited instances, even when this is found as a compound element, even though to a lesser extent than words that only have social hinders and not etymological or morphological ones. The results appear to show that, although a morphological obstacle is visible, sociolinguistic claims seem to be able to divert these obstacles. This study appears particularly suitable for replication tests over the next few decades, which, if society opens up further to claims of inclusiveness, could further corroborate this trend.Keywords: compounds, gender inflection, Italian, morphology
Procedia PDF Downloads 585128 3D Writing on Photosensitive Glass-Ceramics
Authors: C. Busuioc, S. Jinga, E. Pavel
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Optical lithography is a key technique in the development of sub-5 nm patterns for the semiconductor industry. We have already reported that the best results obtained with respect to direct laser writing process on active media, such as glass-ceramics, are achieved only when the energy of the laser radiation is absorbed in discrete quantities. Further, we need to clarify the role of active centers concentration in silver nanocrystals natural generation, as well as in fluorescent rare-earth nanostructures formation. As a consequence, samples with different compositions were prepared. SEM, AFM, TEM and STEM investigations were employed in order to demonstrate that few nm width lines can be written on fluorescent photosensitive glass-ceramics, these being efficient absorbers. Moreover, we believe that the experimental data will lead to the best choice in terms of active centers amount, laser power and glass-ceramic matrix.Keywords: glass-ceramics, 3D laser writing, optical disks, data storage
Procedia PDF Downloads 3005127 Green Electrochemical Nitration of Bioactive Compounds: Biological Evaluation with Molecular Modelling
Authors: Sara Torabi, Sadegh Khazalpour, Mahdi Jamshidi
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Nitro aromatic compounds are valuable materials because of their applications in the preparation of chemical intermediates for the synthesis of dyes, plastics, perfumes, energetic materials, and pharmaceuticals. Chemical and electrochemical procedures are reported for nitration of aromatic compounds. Flavonoid derivatives are present in many vegetables and fruits and are constituent of many common pharmaceuticals and dietary supplements. Electrochemistry provides very versatile means for the electrosynthesis, mechanistic and kinetic studies. To the best of our knowledge, and despite the importance of these compounds in numerous scientific fields, there are no reports on the electrochemical nitration of Quercetin derivatives. Herein, we describe a green electrochemical synthesis of a nitro compound. In this work, electrochemical oxidation of Quercetin has been studied in the presence of nitrite ion as a nucleophile in acetate buffer solution (c = 0.2 M, pH = 6.0), by means of cyclic voltammetry and controlled-potential coulometry. The results indicate the participation of produced o-benzoquinones in Michael reaction with nitrite ion (in the divided cell) to form the corresponding nitro diol (EC mechanism). The purity of product and characterization was done using ¹H NMR, ¹³C NMR, FTIR spectroscopic techniques. The presented strategies use a water/ethanol mixture as solvent. Ethanol as cosolvent was also used in the previous studies because of its low cost, safety, easy availability, recyclability, bioproductability, and biodegradability. These strategies represent a one-pot and facile process for the synthesis of nitro compound in high yield and purity under green conditions.Keywords: electrochemical synthesis, green chemistry, cyclic voltammetry, molecular docking
Procedia PDF Downloads 1465126 ZVZCT PWM Boost DC-DC Converter
Authors: Ismail Aksoy, Haci Bodur, Nihan Altintaş
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This paper introduces a boost converter with a new active snubber cell. In this circuit, all of the semiconductor components in the converter softly turns on and turns off with the help of the active snubber cell. Compared to the other converters, the proposed converter has advantages of size, number of components and cost. The main feature of proposed converter is that the extra voltage stresses do not occur on the main switches and main diodes. Also, the current stress on the main switch is acceptable level. Moreover, the proposed converter can operates under light load conditions and wide input line voltage. In this study, the operating principle of the proposed converter is presented and its operation is verified with the Proteus simulation software for a 1 kW and 100 kHz model.Keywords: active snubber cell, boost converter, zero current switching, zero voltage switching
Procedia PDF Downloads 10275125 Potentiometric Determination of Moxifloxacin in Some Pharmaceutical Formulation Using PVC Membrane Sensors
Authors: M. M. Hefnawy, A. M. A. Homoda, M. A. Abounassif, A. M. Alanazia, A. Al-Majed, Gamal A. E. Mostafa
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PVC membrane sensors using different approach e.g. ion-pair, ionophore, and Schiff-base has been used as testing membrane sensor. Analytical applications of membrane sensors for direct measurement of variety of different ions in complex biological and environmental sample are reported. The most important step of such PVC membrane sensor is the sensing active material. The potentiometric sensors have some outstanding advantages including simple design, operation, wide linear dynamic range, relative fast response time, and rotational selectivity. The analytical applications of these techniques to pharmaceutical compounds in dosage forms are also discussed. The construction and electrochemical response characteristics of Poly (vinyl chloride) membrane sensors for moxifloxacin HCl (MOX) are described. The sensing membranes incorporate ion association complexes of moxifloxacin cation and sodium tetraphenyl borate (NaTPB) (sensor 1), phosphomolybdic acid (PMA) (sensor 2) or phosphotungstic acid (PTA) (sensor 3) as electroactive materials. The sensors display a fast, stable and near-Nernstian response over a relative wide moxifloxacin concentration range (1 ×10-2-4.0×10-6, 1 × 10-2-5.0×10-6, 1 × 10-2-5.0×10-6 M), with detection limits of 3×10-6, 4×10-6 and 4.0×10-6 M for sensor 1, 2 and 3, respectively over a pH range of 6.0-9.0. The sensors show good discrimination of moxifloxacin from several inorganic and organic compounds. The direct determination of 400 µg/ml of moxifloxacin show an average recovery of 98.5, 99.1 and 98.6 % and a mean relative standard deviation of 1.8, 1.6 and 1.8% for sensors 1, 2, and 3 respectively. The proposed sensors have been applied for direct determination of moxifloxacin in some pharmaceutical preparations. The results obtained by determination of moxifloxacin in tablets using the proposed sensors are comparable favorably with those obtained using the US Pharmacopeia method. The sensors have been used as indicator electrodes for potentiometric titration of moxifloxacin.Keywords: potentiometry, PVC, membrane sensors, ion-pair, ionophore, schiff-base, moxifloxacin HCl, sodium tetraphenyl borate, phosphomolybdic acid, phosphotungstic acid
Procedia PDF Downloads 4415124 DNA Intercalating Alkaloids Isolated from Chelidonium majus (Papaveraceae)
Authors: Mohamed Tamer, Wink Michael
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DNA intercalating agents increase the stability of DNA which can be demonstrated by measuring the melting temperature Tm. Tm can be determined in a spectrophotometer in which the cell temperature is increased gradually. The resulting absorption data comes as a sigmoidal curve from which melting temperature can be determined when half of the DNA has denatured. The current study aims to assess DNA intercalating activities of four pure bioactive isoquinoline alkaloids: sanguinarine, berberine, allocryptopine, and chelerythrine which were isolated from Chelidonium majus (Papaveraceae) by repeated silica gel column chromatography, recrystallization and preparative TLC. The isolated compounds were identified by comparing their physical properties and mass spectra with those of the published data. The results showed that sanguiarine is the most active intercalating agent with Tm value of 83.55 ± 0.49 followed by berberine, chelerythrine, and allocryptopine with Tm values 62.58 ± 0.47, 51.38 ± 0.37 and 50.94 ± 0.65, respectively, relative to 49.78 ± 1.05 of bacteriophage DNA alone and 86.09 ± 0.5 for ethidium bromide as a positive control.Keywords: alkaloids, Chelidonium majus, DNA intercalation, Tm
Procedia PDF Downloads 5025123 Tocilizumab Suppresses the Pro-carcinogenic Effects of Breast Cancer-associated Fibroblasts Through Inhibition of the STAT3/AUF1 Pathway
Authors: Naif Al-Jomah, Falah H Al-Mohanna, Abdelilah Aboussekhra
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Active breast cancer-associated fibroblasts (CAFs), the most influential cells in breast tumor microenvironment, express/secrete high levels of the proinvasive/metastatic interleukin-6 (IL-6). Therefore, we have tested here the effect of the IL-6 receptor (IL-6R) inhibitor tocilizumab (TCZ; Actemra) on different active breast CAFs. We have shown that TCZ potently and persistently suppresses the expression of various CAF biomarkers, namely α-SMA, SDF-1 as well as the STAT3 pathway and its downstream target AUF1. TCZ also inhibited the proliferation, migration and invasion abilities of active breast CAF cells. Additionally, TCZ repressed the ability of CAF cells in promoting epithelial-to-mesenchymal transition, and enhancing the migratory/invasive and proliferative capacities of breast cancer cells in vitro. Importantly, these findings were confirmed in orthotopic humanized breast tumors in mice. Furthermore, TCZ suppressed the expression of the pro-angiogenic factor VEGF-A and its transactivator HIF-1α in CAF cells, and consequently inhibited the angiogenic-promoting effect of active CAFs both in vitro and in orthotopic tumor xenografts. These results indicate that inhibition of the IL-6/STAT3/AUF1 pathway by TCZ can normalize active breast CAFs and suppress their paracrine pro-carcinogenic effects, which paves the way toward development of specific CAF-targeting therapy, badly needed for more efficient breast cancer treatments.Keywords: angiogenesis, interleukin-6, paracrine, cancer-associated fibroblasts
Procedia PDF Downloads 985122 Development and Characterization of Expandable TPEs Compounds for Footwear Applications
Authors: Ana Elisa Ribeiro Costa, Sónia Daniela Ferreira Miranda, João Pedro De Carvalho Pereira, João Carlos Simões Bernardo
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Elastomeric thermoplastics (TPEs) have been widely used in the footwear industry over the years. Recently this industry has been requesting materials that can combine lightweight and high abrasion resistance. Although there are blowing agents on the market to improve the lightweight, when these are incorporated into molten polymers during the extrusion or injection molding, it is necessary to have some specific processing conditions (e.g. effect of temperature and hydrodynamic stresses) to obtain good properties and acceptable surface appearance on the final products. Therefore, it is a great advantage for the compounder industry to acquire compounds that already include the blowing agents. In this way, they can be handled and processed under the same conditions as a conventional raw material. In this work, the expandable TPEs compounds, namely a TPU and a SEBS, with the incorporation of blowing agents, have been developed through a co-rotating modular twin-screw parallel extruder. Different blowing agents such as thermo-expandable microspheres and an azodicarbonamide were selected and different screw configurations and temperature profiles were evaluated since these parameters have a particular influence on the expansion inhibition of the blowing agents. Furthermore, percentages of incorporation were varied in order to investigate their influence on the final product properties. After the extrusion of these compounds, expansion was tested by the injection process. The mechanical and physical properties were characterized by different analytical methods like tensile, flexural and abrasive tests, determination of hardness and density measurement. Also, scanning electron microscopy (SEM) was performed. It was observed that it is possible to incorporate the blowing agents on the TPEs without their expansion on the extrusion process. Only with reprocessing (injection molding) did the expansion of the agents occur. These results are corroborated by SEM micrographs, which show a good distribution of blowing agents in the polymeric matrices. The other experimental results showed a good mechanical performance and its density decrease (30% for SEBS and 35% for TPU). This study suggested that it is possible to develop optimized compounds for footwear applications (e.g., sole shoes), which only will be able to expand during the injection process.Keywords: blowing agents, expandable thermoplastic elastomeric compounds, low density, footwear applications
Procedia PDF Downloads 2095121 N₂O₂ Salphen-Like Ligand and Its Pd(II), Ag(I) and Cu(II) Complexes as Potentially Anticancer Agents: Design, Synthesis, Antimicrobial, CT-DNA Binding and Molecular Docking
Authors: Laila H. Abdel-Rahman, Mohamed Shaker S. Adam, Ahmed M. Abu-Dief, Hanan El-Sayed Ahmed
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In this investigation, Cu(II), Pd(II) and Ag(I) complexes with the tetra-dentate DSPH Schiff base ligand were synthesized. The DSPH Schiff base and its complexes were characterized by using different physicochemical and spectral analysis. The results revealed that the metal ions coordinated with DSPH ligand through azomethine nitrogen and phenolic oxygen. Cu(II), Pd(II) and Ag(I) complexes are present in a 1:1 molar ratio. Pd(II) and Ag(I) complexes have square planar geometries while, Cu(II) has a distorted octahedral (Oh) geometry. All investigated complexes are nonelectrolytes. The investigated compounds were tested against different strains of bacteria and fungi. Both prepared compounds showed good results of inhibition against the selected pathogenic microorganism. Moreover, the interaction of investigated complexes with CT-DNA was studied via various techniques and the binding modes are mainly intercalative and grooving modes. Operating Environment MOE package was used to do docking studies for the investigated complexes to explore the potential binding mode and energy. Furthermore, the growth inhibitory effect of the investigated compounds was examined on some cancer cells lines.Keywords: tetradentate, antimicrobial, CT-DNA interaction, docking, anticancer
Procedia PDF Downloads 2445120 Effectiveness of Active Learning in Social Science Courses at Japanese Universities
Authors: Kumiko Inagaki
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In recent, years, Japanese universities have begun to face a dilemma: more than half of all high school graduates go on to attend an institution of higher learning, overwhelming Japanese universities accustomed to small student bodies. These universities have been forced to embrace qualitative changes to accommodate the increased number and diversity of students who enter their establishments, students who differ in their motivations for learning, their levels of eagerness to learn, and their perspectives on the future. One of these changes is an increase in awareness among Japanese educators of the importance of active learning, which deepens students’ understanding of course material through a range of activities, including writing, speaking, thinking, and presenting, in addition to conventional “passive learning” methods such as listening to a one-way lecture. The purpose of this study is to examine the effectiveness of the teaching method adapted to improve active learning. A teaching method designed to promote active learning was implemented in a social science course at one of the most popular universities in Japan. A questionnaire using a five-point response format was given to students in 2,305 courses throughout the university to evaluate the effectiveness of the method based on the following measures: ① the ratio of students who were motivated to attend the classes, ② the rate at which students learned new information, and ③ the teaching method adopted in the classes. The results of this study show that the percentage of students who attended the active learning course eagerly, and the rate of new knowledge acquired through the course, both exceeded the average for the university, the department, and the subject area of social science. In addition, there are strong correlations between teaching method and student motivation and between teaching method and knowledge acquisition rate. These results indicate that the active learning teaching method was effectively implemented and that it may improve student eagerness to attend class and motivation to learn.Keywords: active learning, Japanese university, teaching method, university education
Procedia PDF Downloads 1965119 Evaluation of the Diagnostic Potential of IL-2 after Specific Antigen Stimulation with PE35 (Rv3872) and PPE68 (Rv3873) for the Discrimination of Active and Latent Tuberculosis
Authors: Shima Mahmoudi, Babak Pourakbari, Setareh Mamishi, Mostafa Teymuri, Majid Marjani
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Although cytokine analysis has greatly contributed to the understanding of tuberculosis (TB) pathogenesis, data on cytokine profiles that might distinguish progression from latency of TB infection are scarce. Since PE/PPE proteins are known to induce strong humoral and cellular immune responses, the aim of this study was to evaluate the diagnostic potential of interleukin-2 (IL-2) as biomarker after specific antigen stimulation with PE35 and PPE68 for the discrimination of active and latent tuberculosis infection (LTBI). The production of IL-2 was measured in the antigen-stimulated whole-blood supernatants following stimulation with recombinant PE35 and PPE68. All the patients with active TB and LTBI had positive QuantiFERON-TB Gold in Tube test. The level of IL-2 following stimulation with recombinant PE35 and PPE68 were significantly higher in LTBI group than in patients with active TB infection or control group. The discrimination performance (assessed by the area under ROC curve) for IL-2 following stimulation with recombinant PE35 and PPE68 between LTBI and patients with active TB were 0.837 (95%CI: 0.72-0.97) and 0.75 (95%CI: 0.63-0.89), respectively. Applying the 12.4 pg/mL cut-off for IL-2 induced by PE35 in the present study population resulted in sensitivity of 78%, specificity of 78%, PPV of 78% and NPV of 100%. In addition, a sensitivity of 81%, specificity of 70%, PPV of 67% and 87% of NPV was reported based on the 4.4 pg/mL cut-off for IL-2 induced by PPE68. In conclusion, peptides of the antigen PE35 and PPE68, absent from commonly used BCG strains, stimulated strong IL-2- positive T cell responses in patients with LTBI. This study confirms IL-2 induced by PE35 and PPE68 as a sensitive and specific biomarker and highlights IL-2 as new promising adjunct markers for discriminating of LTBI and Active TB infection.Keywords: IL-2, PE35, PPE68, tuberculosis
Procedia PDF Downloads 4095118 Russian ‘Active Measures’: An Applicable Supporting Tool for Russia`s Foreign Policy Objectives in the 21st Century
Authors: Håkon Riiber
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This paper explores the extent to which Russian ‘Active Measures’ play a role in contemporary Russian foreign policy and in what way the legacy of the Soviet Union is still apparent in these practices. The analysis draws on a set of case studies from the 21st century to examine these aspects, showing which ‘Active Measures’ features are old and which are new in the post-Cold War era. The paper highlights that the topic has gained significant academic and political interest in recent years, largely due to the aggressive posture of the Russian Federation on the world stage, exemplified through interventions in Estonia, Georgia, and Ukraine and interference in several democratic elections in the West. However, the paper argues that the long-term impact of these measures may have unintended implications for Russia. While Russia is unlikely to stop using Active Measures, increased awareness of the exploitation of weaknesses, institutions, or other targets may lead to greater security measures and an ability to identify and defend against these activities. The paper contends that Soviet-style ‘Active Measures’ from the Cold War era have been modernized and are now utilized to create an advantageous atmosphere for further exploitation to support contemporary Russian foreign policy. It offers three key points to support this argument: the reenergized legacy of the Cold War era, the use of ‘Active Measures’ in a number of cases in the 21st century, and the applicability of AM to the Russian approach to foreign policy. The analysis reveals that while this is not a new Russian phenomenon, it is still oversimplified and inaccurately understood by the West, which may result in a decreased ability to defend against these activities and limit the unwarranted escalation of the ongoing security situation between the West and Russia. The paper concludes that the legacy of Soviet-era Active Measures continues to influence Russian foreign policy, and modern technological advances have only made them more applicable to the current political climate. Overall, this paper sheds light on the important issue of Russian ‘Active Measures’ and the role they play in contemporary Russian foreign policy. It emphasizes the need for increased awareness, understanding, and security measures to defend against these activities and prevent further escalation of the security situation between the West and Russia.Keywords: Russian espionage, active measures, disinformation, Russian intelligence
Procedia PDF Downloads 1045117 Volatile Organic Compounds Detection by Surface Acoustic Wave Sensors with Nanoparticles Embedded in Polymer Sensitive Layers
Authors: Cristian Viespe, Dana Miu
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Surface acoustic wave (SAW) sensors with nanoparticles (NPs) of various dimensions and concentrations embedded in different types of polymer sensing films for detecting volatile organic compounds (VOCs) were studied. The sensors were ‘delay line’ type with a center frequency of 69.4 MHz on ST-X quartz substrates. NPs with different diameters of 7 nm or 13 nm were obtained by laser ablation with lasers having 5 ns or 10 ps pulse durations, respectively. The influence of NPs dimensions and concentrations on sensor properties such as frequency shift, sensitivity, noise and response time were investigated. To the best of our knowledge, the influence of NP dimensions on SAW sensor properties with has not been investigated. The frequency shift and sensitivity increased with increasing NP concentration in the polymer for a given NP dimension and with decreasing NP diameter for a given concentration. The best performances were obtained for the smallest NPs used. The SAW sensor with NPs of 7 nm had a limit of detection (LOD) of 65 ppm (almost five times better than the sensor with polymer alone), and a response time of about 9 s for ethanol.Keywords: surface acoustic wave sensor, nanoparticles, volatile organic compounds, laser ablation
Procedia PDF Downloads 1515116 Environmentally Benign Synthesis of 2-Pyrazolines and Cyclohexenones Incorporating Naphthalene Moiety and Their Antimicrobial Evaluation
Authors: Al-Bogami Abdullah Saad
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We reported the environmental benign synthesis of chalcones, 2-pyrazolines and cyclohexanones under microwave irradiation. Chalcones were obtained by the condensation of each of 2-hydroxyacetophenone derivatives with α-naphthaldehyde under microwave irradiation. The condensation reactions of each of synthesized chalcones with phenyl hydrazine under microwave irradiation in the presence of dry acetic acid as a cyclizing agent gave 2-pyrazolines. Also, the new cyclohexenone derivatives, valuable intermediates to synthesize fused heterocycles, have been prepared by the cyclocondensation of each of hydroxychalcones with ethyl acetoacetate. The structures of the synthesized compounds were elucidated by Infrared (IR) spectrometry, Nuclear Magnetic Resonance (NMR), Mass Spectrometry(MS) and elmental analysis. The results indicate that unlike classical heating, microwave irradiation results in higher yields with shorter and cleaner reactions. The synthesized compounds were screened for antimicrobial activity against Staphylococcus aureus, Escherichia coli, Candida Albicans and Aspergillus niger. We clarified the effects of different substituents in the tested compounds on the obtaind antibacterial activities and antifungal activities.Keywords: microwave irradiation, 2-Hydroxyacetophenone, α-Naphthaldehyde, pyrazoline, cyclohexenone, antimicrobial activity
Procedia PDF Downloads 3415115 The Chemical Composition and Larvicidal Activity of Essential Oils Derived from Piper Longepetiolatum and Piper Brachypetiolatum (Piperaceae) Against Aedes Aegypti Larvae (Culicidae) Were Investigated
Authors: Suelen C. Lima, André C. de Oliveira, Rosemary A. Roque
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Dengue is fatal arboviruses transmitted by the A. aegypti mosquito to more than 100 countries, for which the WHO estimates that 2.5 million people will be infected by these disease. The widespread of these diseases is due, among other factors, to the resistance that A. aegypti has to several commercial insecticides. On the other hand, natural products based on plants of the genus Piper (Piperaceae) are characterized by their insecticidal activities against mosquitoes. Piper longepetiolatum and Piper brachypetiolatum are species with wide distribution in the State of Amazonas. However, there is no investigation of phytochemical or biological of these plants against mosquitoes such as A. aegypti. The main of this study was to identify the chemical composition of the essential oil (EOs) from P. longepetiolatum and P. brachypetiolatum and to evaluate the biological activity against A. aegypti. The EOs were extracted by hydrodistillation from leaves (200 g) of P. longepetiolatum and P. brachypetiolatum and analyzed by GC-MS and GC-FID. The main compounds β-caryophyllene (99.9% of purity) and E-nerolidol (99.4% of purity) were purchased from Sigma-Aldrich® Brazil. The larvicidal activity of EOs (20 to 100 ppm), β-caryophyllene and E-nerolidol (10 to 50 ppm) was performed according to WHO protocol against A. aegypti larvae. The GC-MS and GC-FID analysis of EOs from P. longepetiolatum and P. brachypetiolatum indicated the majority presence of β-caryophyllene (35.42%) and E-nerolidol (49.79%), respectively. The results showed that all natural products presented larvicidal activity against A. aegypti. In this aspect, the OE from P. brachypetiolatum (LC50 of 15.51 ppm and LC90 of 22.79 ppm) was more active than the OE from P. longepetiolatum (LC50 of 47.17 ppm and LC90 of 69.60 ppm) (p < 0.05). Regarding of main compounds, E-nerolidol (LC50 of 9.50 ppm and LC90 of 23.89 ppm) showed higher larvicidal activity than the β-caryophyllene compound (LC50 of 79.00 ppm and LC90 of 230.91 ppm) (p < 0.05). The larvae treated with these natural products showed tremors and lethargic movements, suggesting that these natural products have neurotoxic action. These observations support studies to investigate the mechanism of action. This is the first record of the chemical composition and larvicidal activity of the EO from P. longepetiolatum and P. brachypetiolatum rich in β-caryophyllene and E-nerolidol against A. aegypti larvae.Keywords: piperaceae, aedes, sesquiterpenes, biological control
Procedia PDF Downloads 775114 Discerning of Antimicrobial Potential of Phenylpropanoic Acid Derived Oxadiazoles
Authors: Neeraj Kumar Fuloria, Shivkanya Fuloria, Amit Singh
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2-Phenyl propionic acid and oxadiazoles possess antimicrobial potential. 2-Phenyl propane hydrazide (1), on cyclization with aromatic acids offered 2-aryl-5-(1-phenylethyl)-1,3,4-oxadiazole derivatives (1A-E). The PPA derived oxadiazoles were characterized by elemental analysis and spectral studies. The compounds were screened for antimicrobial potential. The compound 1D bearing strong electron withdrawing group showed maximum antimicrobial potential. Other compounds also displayed antimicrobial potential to a certain extent. The SAR of newer oxadiazoles indicated that substitution of strong electronegative group in the PPA derived oxadiazoles enhanced their antimicrobial potential.Keywords: antimicrobial, imines, oxadiazoles, PPA
Procedia PDF Downloads 3425113 An Active Rectifier with Time-Domain Delay Compensation to Enhance the Power Conversion Efficiency
Authors: Shao-Ku Kao
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This paper presents an active rectifier with time-domain delay compensation to enhance the efficiency. A delay calibration circuit is designed to convert delay time to voltage and adaptive control on/off delay in variable input voltage. This circuit is designed in 0.18 mm CMOS process. The input voltage range is from 2 V to 3.6 V with the output voltage from 1.8 V to 3.4 V. The efficiency can maintain more than 85% when the load from 50 Ω ~ 1500 Ω for 3.6 V input voltage. The maximum efficiency is 92.4 % at output power to be 38.6 mW for 3.6 V input voltage.Keywords: wireless power transfer, active diode, delay compensation, time to voltage converter, PCE
Procedia PDF Downloads 2835112 Study of Bis(Trifluoromethylsulfonyl)Imide Based Ionic Liquids by Gas Chromatography
Authors: F. Mutelet, L. Cesari
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Development of safer and environmentally friendly processes and products is needed to achieve sustainable production and consumption patterns. Ionic liquids, which are of great interest to the chemical and related industries because of their attractive properties as solvents, should be considered. Ionic liquids are comprised of an asymmetric, bulky organic cation and a weakly coordinating organic or inorganic anion. A large number of possible combinations allows for the ability to ‘fine tune’ the solvent properties for a specific purpose. Physical and chemical properties of ionic liquids are not only influenced by the nature of the cation and the nature of cation substituents but also by the polarity and the size of the anion. These features infer to ionic liquids numerous applications, in organic synthesis, separation processes, and electrochemistry. Separation processes required a good knowledge of the behavior of organic compounds with ionic liquids. Gas chromatography is a useful tool to estimate the interactions between organic compounds and ionic liquids. Indeed, retention data may be used to determine infinite dilution thermodynamic properties of volatile organic compounds in ionic liquids. Among others, the activity coefficient at infinite dilution is a direct measure of solute-ionic liquid interaction. In this work, infinite dilution thermodynamic properties of volatile organic compounds in specific bis(trifluoromethylsulfonyl)imide based ionic liquids measured by gas chromatography is presented. It was found that apolar compounds are not miscible in this family of ionic liquids. As expected, the solubility of organic compounds is related to their polarity and hydrogen-bond. Through activity coefficients data, the performance of these ionic liquids was evaluated for different separation processes (benzene/heptane, thiophene/heptane and pyridine/heptane). Results indicate that ionic liquids may be used for the extraction of polar compounds (aromatics, alcohols, pyridine, thiophene, tetrahydrofuran) from aliphatic media. For example, 1-benzylpyridinium bis(trifluoromethylsulfonyl) imide and 1-cyclohexylmethyl-1-methylpyrrolidinium bis(trifluoromethylsulfonyl)imide are more efficient for the extraction of aromatics or pyridine from aliphatics than classical solvents. Ionic liquids with long alkyl chain length present important capacity values but their selectivity values are low. In conclusion, we have demonstrated that specific bis(trifluoromethylsulfonyl)imide based ILs containing polar chain grafted on the cation (for example benzyl or cyclohexyl) increases considerably their performance in separation processes.Keywords: interaction organic solvent-ionic liquid, gas chromatography, solvation model, COSMO-RS
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