Search results for: bioactive compounds interaction
3685 Tenofovir-Amino Acid Conjugates Act as Polymerase Substrates: Implications for Avoiding Cellular Phosphorylation in the Discovery of Nucleotide Analogs
Authors: Weijie Gu, Sergio Martinez, Hoai Nguyen, Hongtao Xu, Piet Herdewijn, Steven De Jonghe, Kalyan Das
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Nucleotide analogs are used for treating viral infections such as HIV, hepatitis B, hepatitis C, influenza, and SARS-CoV-2. To become polymerase substrates, a nucleotide analog must be phosphorylated by cellular kinases, which are rate-limiting. The goal of this study is to develop dNTP/NTP analogs directly from nucleotides. Tenofovir (TFV) analogs were synthesized by conjugating with natural or unnatural amino acids. It demonstrates that some conjugates act as dNTP analogs, and HIV-1 reverse transcriptase (RT) catalytically incorporates the TFV part as the chain terminator. X-ray structures in complex with HIV-1 RT/dsDNA showed binding of the conjugates at the polymerase active site, however, in different modes in the presence of Mg²⁺ vs. Mn²⁺ ions. The adaptability of the compounds is seemingly essential for catalytic incorporation of TFV by RT. 4d with a carboxyl sidechain demonstrated the highest incorporation. 4e showed weak incorporation and rather behaved as a dNTP-competitive inhibitor. This result advocates the feasibility of designing NTP/dNTP analogs by chemical substitutions to nucleotide analogs.Keywords: dNTP analogs, nucleotide analogs, polymerase, tenofovir, X-ray structure
Procedia PDF Downloads 1533684 Improving the Technology of Assembly by Use of Computer Calculations
Authors: Mariya V. Yanyukina, Michael A. Bolotov
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Assembling accuracy is the degree of accordance between the actual values of the parameters obtained during assembly, and the values specified in the assembly drawings and technical specifications. However, the assembling accuracy depends not only on the quality of the production process but also on the correctness of the assembly process. Therefore, preliminary calculations of assembly stages are carried out to verify the correspondence of real geometric parameters to their acceptable values. In the aviation industry, most calculations involve interacting dimensional chains. This greatly complicates the task. Solving such problems requires a special approach. The purpose of this article is to carry out the problem of improving the technology of assembly of aviation units by use of computer calculations. One of the actual examples of the assembly unit, in which there is an interacting dimensional chain, is the turbine wheel of gas turbine engine. Dimensional chain of turbine wheel is formed by geometric parameters of disk and set of blades. The interaction of the dimensional chain consists in the formation of two chains. The first chain is formed by the dimensions that determine the location of the grooves for the installation of the blades, and the dimensions of the blade roots. The second dimensional chain is formed by the dimensions of the airfoil shroud platform. The interaction of the dimensional chain of the turbine wheel is the interdependence of the first and second chains by means of power circuits formed by a plurality of middle parts of the turbine blades. The timeliness of the calculation of the dimensional chain of the turbine wheel is the need to improve the technology of assembly of this unit. The task at hand contains geometric and mathematical components; therefore, its solution can be implemented following the algorithm: 1) research and analysis of production errors by geometric parameters; 2) development of a parametric model in the CAD system; 3) creation of set of CAD-models of details taking into account actual or generalized distributions of errors of geometrical parameters; 4) calculation model in the CAE-system, loading of various combinations of models of parts; 5) the accumulation of statistics and analysis. The main task is to pre-simulate the assembly process by calculating the interacting dimensional chains. The article describes the approach to the solution from the point of view of mathematical statistics, implemented in the software package Matlab. Within the framework of the study, there are data on the measurement of the components of the turbine wheel-blades and disks, as a result of which it is expected that the assembly process of the unit will be optimized by solving dimensional chains.Keywords: accuracy, assembly, interacting dimension chains, turbine
Procedia PDF Downloads 3733683 The Zen Socrates Archetype and the Priority of the Unanswerable Question
Authors: Shawn Thompson
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Socrates and Zen Buddhism are separated by time, distance, and cultures in a way that it is unlikely that they influenced each other. And yet the two have an amazing similarity in the principle that paradoxical and unanswerable questions can be a form of wisdom that produces a healthy psyche. Both have a sense that the limit of human awareness is a wisdom of this uncertainty. Both are at odds with the dogma of answers and of a western rationality that prioritizes the answer. Both have enigmatic answers that perpetuate the question. Both use the form of a dialogue of interaction with mutual illumination rather than the form of a lecture to passive recipients. If these premises are true, Socrates and Zen Buddhism has elements in common that reflect basic human needs for a good life. It can be argued that there is a joint archetypal experience of the wisdom of uncertainty and unanswerable questions in Socrates and Zen Buddhism.Keywords: zen buddhism, socrates, unanswerable questions, aporia
Procedia PDF Downloads 753682 Exploration of the Possible Link Between Emotional Problems and Cholesterol Levels Among Children Diagnosed with Attention-Deficit Hyperactivity Disorder
Authors: Rosa S. Wong, Keith T.S. Tung, H.W. Tsang, Frederick K. Ho, Patrick Ip
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Attention-deficit hyperactivity disorder (ADHD) is a neurodevelopmental disorder characterized by inattention and hyperactive-impulsive behavior. Evidence shows that ADHD and mood problems such as depression and anxiety often co-occur and yet not everyone with ADHD reported elevated emotional problems. Given that cholesterol is essential for healthy brain development including the regions governing emotion regulation, reports found lower cholesterol levels in patients with major depressive disorder and those with suicide attempt behavior compared to healthy subjects. This study explored whether ADHD adolescents experienced more emotional problems and whether emotional problems correlated with cholesterol levels in these adolescents. This study used a portion of data from the longitudinal cohort study which was designed to investigate the long-term impact of family socioeconomic status on child development. In 2018/19, parents of 300 adolescents (average age: 12.57+/-0.49 years) were asked to rate their children’s emotional problems and report whether their children had doctor-diagnosed psychiatric diseases. We further collected blood samples from 263 children to study their lipid profile (total cholesterol, high-density lipoprotein (HDL)-cholesterol, and low-density lipoprotein (LDL)-cholesterol). Regression analyses were performed to test the relationships between variables of interest. Among 300 children, 27 (9%) had ADHD diagnosis. Analysis based on overall sample found no association between ADHD and emotional problems, but when investigating the relationship by gender, there was a significant interaction effect of ADHD and gender on emotional problems (p=0.037), with ADHD males displaying more emotional problems than ADHD females. Further analyses based on 263 children (21 with ADHD diagnosis) found significant interaction effect of ADHD and gender on total cholesterol (p=0.038) and low LDL-cholesterol levels (p=0.013) after adjusting for the child’s physical disease history. Specifically, ADHD males had significantly lower total cholesterol and low lipoprotein-cholesterol levels than ADHD females. In ADHD males, more emotional problems were associated with lower LDL-cholesterol levels (B = -4.26, 95%CI (-7.46, -1.07), p=0.013). We found preliminary support for the association between more emotional problems and lower cholesterol levels in ADHD children, especially among males. Although larger prospective studies are needed to substantiate these claims, the evidence highlights the importance of healthy lifestyle to keep cholesterol levels in normal range which can have positive effects on physical and mental health.Keywords: attention-deficit hyperactivity disorder, cholesterol, emotional problems, adolescents
Procedia PDF Downloads 1493681 Total Phenols, Total Flavonoids Contents and Free Radical Scavenging Activity of Seeds Extracts of Lawsonia alba (henna) from Algeria
Authors: Rekia. Cherbi, Mokhtar. Saidi, Mohamed. Yousfi, Zhor. Rahmani
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Lawsonia alba (Henna) is widely used in folkloric medicinal for a treatment of various skin diseases such as Eczema (atopic dermatitis), boils and sores. The aim of the present study is to determine the antioxidant activity, total phenolics, flavonoids, and condensed tannins content of extracts from the seeds of Lawsonia. alba grown in Algeria and selected from three different regions (Adrar, Biskra, and Ouargla). Total phenolics content ranged from 68,42 ± 0,54 to 88,31 ± 0,78mg gallic acid equivalents (GAE)/g dry weight, the flavonoids content varied from 1,13 ± 0,0035 to 1,367 ± 0,002mg quercetin equivalents (Q)/ g dry weight and condensed tannins (14,47 ± 0,138 to 25,50 ± 0,076 mg catechin equivalents (CE)/g dry weight). The antioxidant activities of the extracts were evaluated by DPPH assay. The results showed that all extracts from the seeds of Lawsonia. alba seem to be good trappers of radicals, the IC50 values of the extracts ranged between 0,00826 and 0,01 g/l.Keywords: antioxidant activity, Lawsonia. alba, phenolic compounds, seeds
Procedia PDF Downloads 3473680 Suitable Indoor Plants for Green Office Development in Faculty of Science and Technology, Suan Sunandha Rajabhat University, Thailand
Authors: Tatsanawalai Utarasakul
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Nowadays, green office principles are very broadly initiated in many offices, organizations, as well as in universities. The concepts of green office are composed of seven prominent issues. One of them, physical implementation, is to develop a pleasant atmosphere for staff in the faculty with selected optimum plant species for the office. 50 species from NASA research and other documents were studied for the selection criteria of plants which were appropriate for specific locations in order to reduce indoor air pollutants such as formaldehyde, benzene, and trichloroethylene. For the copy and examination preparation room in which particulate matter and volatile organic compounds can be found, some plants such as peace lily, gerbera daisy, and bamboo palm should be set, which are very effective in treating trichloroethylene. For common rooms and offices where formaldehyde can be found, which is generated from many building materials, bamboo palm, mother-in-law's tongue, peace lily, striped dracaena, cornstalk plant, golden pathos, and green spider plant should be set.Keywords: indoor plants, indoor air quality, phytoremediation, green office
Procedia PDF Downloads 4573679 Experimental Measurements for the Effect of Dilution Procedure in Blood Esterases as Animals Biomarker for Exposure to Organophosphate Compounds
Authors: Kasim Sakran Abass
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This main aim of this study was to confirm and extend our current knowledge about the effects of dilutions on esterases activities in the blood for birds with respect to protecting the enzyme from organophosphate inhibition. There were significantly higher esterases activities in dilution 1:10 in all blood samples from quail, duck, and chick compared to other dilutions (1:5, 1:15, 1:20, and 1:25). Furthermore, our results also pointed to the importance of estimating different dilutions effects prior to using in birds as biomarker tools of environmental exposure. Concentration–inhibition curves were determined for the inhibitor in the presence of dilutions 1:5, 1:10 plus 1:15 (to stimulate carboxylesterase). Point estimates (concentrations calculated to produce 20, 50, and 80% inhibition) were compared across conditions and served as a measure of esterase-mediated detoxification. Among the thiol esters (dilution 1:5) was observed to have the highest specificity constant (kcat/Km), and the Km and kcat values were 176 μM and 16,765 s−1, respectively for S-phenyl thioacetate ester, while detected in (dilution 1:15) the lowest specificity constant (kcat/Km), and the Km and kcat values were 943 μM and 1154 s−1, respectively for acetylthiocholine iodide ester.Keywords: esterase, animal, dilution, pesticides
Procedia PDF Downloads 5283678 Seismic Hazard Assessment of Offshore Platforms
Authors: F. D. Konstandakopoulou, G. A. Papagiannopoulos, N. G. Pnevmatikos, G. D. Hatzigeorgiou
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This paper examines the effects of pile-soil-structure interaction on the dynamic response of offshore platforms under the action of near-fault earthquakes. Two offshore platforms models are investigated, one with completely fixed supports and one with piles which are clamped into deformable layered soil. The soil deformability for the second model is simulated using non-linear springs. These platform models are subjected to near-fault seismic ground motions. The role of fault mechanism on platforms’ response is additionally investigated, while the study also examines the effects of different angles of incidence of seismic records on the maximum response of each platform.Keywords: hazard analysis, offshore platforms, earthquakes, safety
Procedia PDF Downloads 1483677 Disparities in Language Competence and Conflict: The Moderating Role of Cultural Intelligence in Intercultural Interactions
Authors: Catherine Peyrols Wu
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Intercultural interactions are becoming increasingly common in organizations and life. These interactions are often the stage of miscommunication and conflict. In management research, these problems are commonly attributed to cultural differences in values and interactional norms. As a result, the notion that intercultural competence can minimize these challenges is widely accepted. Cultural differences, however, are not the only source of a challenge during intercultural interactions. The need to rely on a lingua franca – or common language between people who have different mother tongues – is another important one. In theory, a lingua franca can improve communication and ease coordination. In practice however, disparities in people’s ability and confidence to communicate in the language can exacerbate tensions and generate inefficiencies. In this study, we draw on power theory to develop a model of disparities in language competence and conflict in a multicultural work context. Specifically, we hypothesized that differences in language competence between interaction partners would be positively related to conflict such that people would report greater conflict with partners who have more dissimilar levels of language competence and lesser conflict with partners with more similar levels of language competence. Furthermore, we proposed that cultural intelligence (CQ) an intercultural competence that denotes an individual’s capability to be effective in intercultural situations, would weaken the relationship between disparities in language competence and conflict such that people would report less conflict with partners who have more dissimilar levels of language competence when the interaction partner has high CQ and more conflict when the partner has low CQ. We tested this model with a sample of 135 undergraduate students working in multicultural teams for 13 weeks. We used a round-robin design to examine conflict in 646 dyads nested within 21 teams. Results of analyses using social relations modeling provided support for our hypotheses. Specifically, we found that in intercultural dyads with large disparities in language competence, partners with the lowest level of language competence would report higher levels of interpersonal conflict. However, this relationship disappeared when the partner with higher language competence was also high in CQ. These findings suggest that communication in a lingua franca can be a source of conflict in intercultural collaboration when partners differ in their level of language competence and that CQ can alleviate these effects during collaboration with partners who have relatively lower levels of language competence. Theoretically, this study underscores the benefits of CQ as a complement to language competence for intercultural effectiveness. Practically, these results further attest to the benefits of investing resources to develop language competence and CQ in employees engaged in multicultural work.Keywords: cultural intelligence, intercultural interactions, language competence, multicultural teamwork
Procedia PDF Downloads 1653676 Quantitative Analysis of Carcinoembryonic Antigen (CEA) Using Micromechanical Piezoresistive Cantilever
Authors: Meisam Omidi, M. Mirijalili, Mohammadmehdi Choolaei, Z. Sharifi, F. Haghiralsadat, F. Yazdian
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In this work, we have used arrays of micromechanical piezoresistive cantilever with different geometries to detect carcinoembryonic antigen (CEA), which is known as an important biomarker associated with various cancers such as the colorectal, lung, breast, pancreatic, and bladder cancer. The sensing principle is based on the surface stress changes induced by antigen–antibody interaction on the microcantilevers surfaces. Different concentrations of CEA in a human serum albumin (HSA) solution were detected as a function of the deflection of the beams. According to the experiments, it was revealed that microcantilevers have surface stress sensitivities in the order of 8 (mJ/m). This matter allows them to detect CEA concentrations as low as 3 ng/mL or 18 pM. This indicates the fact that the self-sensing microcantilever approach is beneficial for pathological tests.Keywords: micromechanical biosensors, carcinoembryonic antigen (CEA), surface stress
Procedia PDF Downloads 4723675 Selenium Content in Agricultural Soils and Wheat from the Balkan Peninsula
Authors: S. Krustev, V. Angelova, P. Zaprjanova
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Selenium (Se) is an essential micro-nutrient for human and animals but it is highly toxic. Its organic compounds play an important role in biochemistry and nutrition of the cells. Concentration levels of this element in the different regions of the world vary considerably. This study aimed to compare the availability and levels of the Se in some rural areas of the Balkan Peninsula and relationship with the concentrations of other trace elements. For this purpose soil samples and wheat grains from different regions of Bulgaria, Serbia, Nord Macedonia, Romania, and Greece situated far from large industrial centers have been analyzed. The main methods for their determination were the atomic spectral techniques – atomic absorption and plasma atomic emission. As a result of this study, data on microelements levels from the main grain-producing regions of the Balkan Peninsula were determined and systematized. The presented results confirm the low levels of Se in this region: 0.222– 0.962 mg.kg-1 in soils and 0.001 - 0.005 mg.kg-1 in wheat grains and require measures to offset the effect of this deficiency.Keywords: agricultural soils, balkan peninsula, rural areas, selenium
Procedia PDF Downloads 1323674 Nonlinear Optical Properties for Three Level Atoms at Resonance and Off-Resonance with Laser Coupled Beams
Authors: Suad M. Abuzariba, Eman O. Mafaa
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For three level atom interacts with a laser beam, the effect of changing resonance and off-resonance frequencies has been studied. Furthermore, a clear distortion has been seen in both the real and imaginary parts of the electric susceptibility with increasing the frequency of the coupled laser beams so that reaching the off-resonance interaction. With increasing the Rabi frequency of the laser pulse that in resonance with the lower transition the distortion will produce a new peak in the electric susceptibility parts, in both the real and imaginary ones.Keywords: electric susceptibility, resonance frequency off-resonance frequency, three level atom, laser
Procedia PDF Downloads 3113673 The Concurrent Effect of Autistic and Schizotypal Traits on Convergent and Divergent Thinking
Authors: Ahmad Abu-Akel, Emilie De Montpellier, Sophie Von Bentivegni, Lyn Luechinger, Alessandro Ishii, Christine Mohr
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Convergent and divergent thinking are two main components of creativity that have been viewed as complementary. While divergent thinking refers to the fluency and flexibility of generating new ideas, convergent thinking refers to the ability to systematically apply rules and knowledge to arrive at the optimal solution or idea. These creativity components have been shown to be susceptible to variation in subclinical expressions of autistic and schizotypal traits within the general population. Research, albeit inconclusively, mainly linked positive schizotypal traits with divergent thinking and autistic traits with convergent thinking. However, cumulative evidence suggests that these trait dimensions can co-occur in the same individual more than would be expected by chance and that their concurrent effect can be diametric and even interactive. The current study aimed at investigating the concurrent effect of these trait dimensions on tasks assessing convergent and divergent thinking abilities. We predicted that individuals with high positive schizotypal traits alone would perform particularly well on the divergent thinking task, whilst those with high autistic traits alone would perform particularly well on the convergent thinking task. Crucially, we also predicted that individuals who are high on both autistic and positive schizotypal traits would perform particularly well on both the divergent and convergent thinking tasks. This was investigated in a non-clinical sample of 142 individuals (Males = 45%; Mean age = 21.45, SD = 2.30), sufficient to minimally observe an effect size f² ≥ .10. Divergent thinking was evaluated using the Alternative Uses Task, and convergent thinking with the Anagrams Task. Autistic and schizotypal traits were respectively assessed with the Autism Quotient Questionnaire (AQ) and the Oxford-Liverpool Inventory of Feelings and Experiences (O-LIFE). Regression analyses revealed that the positive association of autistic traits with convergent thinking scores was qualified with an interaction with positive schizotypal traits. Specifically, positive schizotypal traits were negatively associated with convergent thinking scores when AQ scores were relatively low, but this trend was reversed when AQ scores were high. Conversely, the positive effect of AQ scores on convergent thinking progressively increased with increasing positive schizotypal traits. The results of divergent thinking task are currently being analyzed and will be reported at the conference. The association of elevated autistic and positive schizotypal traits with convergent thinking may represent a unique profile of creative thinkers who are able to simultaneously draw on trait-specific advantages conferred by autistic and positively schizotypal traits such as local and global processing. This suggests that main-effect models can tell an incomplete story regarding the effect of autistic and positive schizotypal traits on creativity-related processes. Future creativity research should consider their interaction and the benefits conferred by their co-presence.Keywords: autism, schizotypy, convergent thinking, divergent thinking, comorbidity
Procedia PDF Downloads 1803672 Prey-Predator Eco-Epidemiological Model with Nonlinear Transmission Disease
Authors: Qamar J. A. Khan, Fatma Ahmed Al Kharousi
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A prey-predator eco-epidemiological model is studied where transmission of the disease between infected and uninfected prey is nonlinear. The interaction of the predator with infected and uninfected prey species depend on their numerical superiority. Harvesting of both uninfected and infected prey is considered. Stability analysis is carried out for equilibrium values. Using the parameter µ, the death rate of infected prey as a bifurcation parameter it is shown that Hopf bifurcation could occur. The theoretical results are compared with numerical results for different set of parameters.Keywords: bifurcation, optimal harvesting, predator, prey, stability
Procedia PDF Downloads 3023671 Improvement in Safety Profile of Semecarpus Anacardium Linn by Shodhana: An Ayurvedic Purification Method
Authors: Umang H. Gajjar, K. M. Khambholja, R. K. Patel
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Semecarpus anacardium shows the presence of bioflavonoids, phenolic compounds, bhilawanols, minerals, vitamins and amino acids. Detoxified S. anacardium and its oils are considered to have anti-inflammatory properties and used in nervous debility, neuritis, rheumatism and leprous modules. S. anacardium if used without purification causes toxic skin inflammation problem because it contains toxic phenolic oil. During this Shodhana Process - An ayurvedic purification method, toxic phenolic oil was removed, have marked effect on the concentration of the phytoconstituent & antioxidant activity of S. anacardium. Total phenolic content decreased up to 70 % (from 28.9 %w/w to 8.94 %w/w), while there is a negligible effect on the concentration of total flavonoid (7.51 %w/w to 7.43 %w/w) and total carbohydrate (0.907 %w/w to 0.853 % w/w) content. IC50& EC50 value of extract of S. anacardium before and after purification are 171.7 & 314.3 while EC50values are 280.μg/ml & 304. μg/ml, shows that antioxidant activity of S. anacardium is decreased but the safety profile of the drug is increased as the toxic phenolic oil was removed during Shodhana - An ayurvedic purification method.Keywords: Semecarpus anacardium, Shodhana process, safety profile, improvement
Procedia PDF Downloads 2573670 Microwave Assisted Extractive Desulfurization of Gas Oil Feedstock
Authors: Hamida Y. Mostafa, Ghada E. Khedr, Dina M. Abd El-Aty
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Sulfur compound removal from petroleum fractions is a critical component of environmental protection demands. Solvent extraction, oxidative desulfurization, or hydro-treatment techniques have traditionally been used as the removal processes. While all methods were capable of eliminating sulfur compounds at moderate rates, they had some limitations. A major problem with these routes is their high running expenses, which are caused by their prolonged operation times and high energy consumption. Therefore, new methods for removing sulfur are still necessary. In the current study, a simple assisted desulfurization system for gas oil fraction has been successfully developed using acetonitrile and methanol as a solvent under microwave irradiation. The key variables affecting sulfur removal have been studied, including microwave power, irradiation time, and solvent to gas oil volume ratio. At the conclusion of the research that is being presented, promising results have been found. The results show that a microwave-assisted extractive desulfurization method had remove sulfur with a high degree of efficiency under the suitable conditions.Keywords: extractive desulfurization, microwave assisted extraction, petroleum fractions, acetonitrile and methanol
Procedia PDF Downloads 1033669 Multiclass Analysis of Pharmaceuticals in Fish and Shrimp Tissues by High-Performance Liquid Chromatography-Tandem Mass Spectrometry
Authors: Reza Pashaei, Reda Dzingelevičienė
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An efficient, reliable, and sensitive multiclass analytical method has been expanded to simultaneously determine 15 human pharmaceutical residues in fish and shrimp tissue samples by ultra-high-performance liquid chromatography-tandem mass spectrometry. The investigated compounds comprise ten classes, namely analgesic, antibacterial, anticonvulsant, cardiovascular, fluoroquinolones, macrolides, nonsteroidal anti-inflammatory, penicillins, stimulant, and sulfonamide. A simple liquid extraction procedure based on 0.1% formic acid in methanol was developed. Chromatographic conditions were optimized, and mobile phase namely 0.1 % ammonium acetate (A), and acetonitrile (B): 0 – 2 min, 15% B; 2 – 5 min, linear to 95% B; 5 – 10 min, 95% B; and 10 – 12 min was obtained. Limits of detection and quantification ranged from 0.017 to 1.371 μg/kg and 0.051 to 4.113 μg/kg, respectively. Finally, amoxicillin, azithromycin, caffeine, carbamazepine, ciprofloxacin, clarithromycin, diclofenac, erythromycin, furosemide, ibuprofen, ketoprofen, naproxen, sulfamethoxazole, tetracycline, and triclosan were quantifiable in fish and shrimp samples.Keywords: fish, liquid chromatography, mass spectrometry, pharmaceuticals, shrimp, solid-phase extraction
Procedia PDF Downloads 2623668 Leveraging the HDAC Inhibitory Pharmacophore to Construct Deoxyvasicinone Based Tractable Anti-Lung Cancer Agent and pH-Responsive Nanocarrier
Authors: Ram Sharma, Esha Chatterjee, Santosh Kumar Guru, Kunal Nepali
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A tractable anti-lung cancer agent was identified via the installation of a Ring C expanded synthetic analogue of the alkaloid vasicinone [7,8,9,10-tetrahydroazepino[2,1-b] quinazolin-12(6H)-one (TAZQ)] as a surface recognition part in the HDAC inhibitory three-component model. Noteworthy to mention that the candidature of TAZQ was deemed suitable for accommodation in HDAC inhibitory pharmacophore as per the results of the fragment recruitment process conducted by our laboratory. TAZQ was pinpointed through the fragment screening program as a synthetically flexible fragment endowed with some moderate cell growth inhibitory activity against the lung cancer cell lines, and it was anticipated that the use of the aforementioned fragment to generate hydroxamic acid functionality (zinc-binding motif) bearing HDAC inhibitors would boost the antitumor efficacy of TAZQ. Consistent with our aim of applying epigenetic targets to the treatment of lung cancer, a strikingly potent anti-lung cancer scaffold (compound 6) was pinpointed through a series of in-vitro experiments. Notably, the compounds manifested a magnificent activity profile against KRAS and EGFR mutant lung cancer cell lines (IC50 = 0.80 - 0.96 µM), and the effects were found to be mediated through preferential HDAC6 inhibition (IC50 = 12.9 nM). In addition to HDAC6 inhibition, the compounds also elicited HDAC1 and HDAC3 inhibitory activity with an IC50 value of 49.9 nM and 68.5 nM, respectively. The HDAC inhibitory ability of compound 6 was also confirmed from the results of the western blot experiment that revealed its potential to decrease the expression levels of HDAC isoforms (HDAC1, HDAC3, and HDAC6). Noteworthy to mention that complete downregulation of the HDAC6 isoform was exerted by compound 6 at 0.5 and 1 µM. Moreover, in another western blot experiment, treatment with hydroxamic acid 6 led to upregulation of H3 acK9 and α-Tubulin acK40 levels, ascertaining its inhibitory activity toward both the class I HDACs and Class II B HDACs. The results of other assays were also encouraging as treatment with compound 6 led to the suppression of the colony formation ability of A549 cells, induction of apoptosis, and increase in autophagic flux. In silico studies led us to rationalize the results of the experimental assay, and some key interactions of compound 6 with the amino acid residues of HDAC isoforms were identified. In light of the impressive activity spectrum of compound 6, a pH-responsive nanocarrier (hyaluronic acid-compound 6 nanoparticles) was prepared. The dialysis bag approach was used for the assessment of the nanoparticles under both normal and acidic circumstances, and the pH-sensitive nature of hyaluronic acid-compound 6 nanoparticles was confirmed. Delightfully, the nanoformulation was devoid of cytotoxicity against the L929 mouse fibroblast cells (normal settings) and exhibited selective cytotoxicity towards the A549 lung cancer cell lines. In a nutshell, compound 6 appears to be a promising adduct, and a detailed investigation of this compound might yield a therapeutic for the treatment of lung cancer.Keywords: HDAC inhibitors, lung cancer, scaffold, hyaluronic acid, nanoparticles
Procedia PDF Downloads 953667 Enhancing Food Security through Cabbage Production by Local Fammers in Nkokobe Municipality
Authors: Sipumle Qapeshu, Bongiwe Mcata, Ajuruchukwu Obi
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Subsistence farmers practice farming for survival while commercial farmers produce to feed themselves and larger society with the motive to achieve highest profit. These types of farmers are characterised by growing what they eat, live without making regular purchases in the markets. The main objective of subsistence/peasant farmers is to ensure food security at household level. Cabbage is a crop that has been identified to have vital food nutrient sources like Vitamin A, B and C, protein, calcium, iron and antioxidative compounds beneficial for preventing cancer. This paper, therefore, looks at the potential that cabbage production has in enhancing household food security and also the challenges encountered by these cabbage producers. Primary data was obtained from 50 respondents, and linear regression model was used to analyse the data used. Income was used as food security measure. The results showed that three variables were statistically significant and they are gender (10%), education (5%) and household size (5%). Meaning that these are variables that influenced cabbage production by these households, and it also affects their food security status since income is affected.Keywords: subsistence farmers, food security, cabbage, farming
Procedia PDF Downloads 3003666 The Effect of Absolute and Relative Deprivation on Homicides in Brazil
Authors: Temidayo James Aransiola, Vania Ceccato, Marcelo Justus
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This paper investigates the effect of absolute deprivation (proxy unemployment) and relative deprivation (proxy income inequality) on homicide levels in Brazil. A database from the Brazilian Information System about Mortality and Census of the year 2000 and 2010 was used to estimate negative binomial models of homicide levels controlling for socioeconomic, demographic and geographic factors. Findings show that unemployment and income inequality affect homicides levels and that the effect of the former is more pronounced compared to the latter. Moreover, the combination of income inequality and unemployment exacerbates the overall effect of deprivation on homicide levels.Keywords: deprivation, inequality, interaction, unemployment, violence
Procedia PDF Downloads 1463665 Correlation Analysis of Reactivity in the Oxidation of Para and Meta-Substituted Benzyl Alcohols by Benzimidazolium Dichromate in Non-Aqueous Media: A Kinetic and Mechanistic Aspects
Authors: Seema Kothari, Dinesh Panday
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An observed correlation of the reaction rates with the changes in the nature of substituent present on one of the reactants often reveals the nature of transition state. Selective oxidation of organic compounds under non-aqueous media is an important transformation in synthetic organic chemistry. Inorganic chromates and dichromates being drastic oxidant and are generally insoluble in most organic solvents, a number of different chromium (VI) derivatives have been synthesized. Benzimidazolium dichromate (BIDC) is one of the recently reported Cr(VI) reagents which is neither hygroscopic nor light sensitive being, therefore, much stable. Not many reports on the kinetics of the oxidations by BIDC are seemed to be available in the literature. In the present investigation, the kinetics and mechanism of benzyl alcohol (BA) and a number of para- and meta-substituted benzyl alcohols by benzimidazolium dichromate (BIDC), in dimethyl sulphoxide, is reported. The reactions were followed spectrophotometrically at 364 nm by monitoring the decrease in [BIDC] for up to 85-90% reaction, the temperature being constant. The observed oxidation product is the corresponding benzaldehyde. The reactions were of first order with respect to each the alcohol and BIDC. The reactions are catalyzed by proton, and the dependence is of the form: kobs = a + b[H+]. The reactions thus follow both, an acid-dependent and acid-independent paths. The oxidation of [1,1 2H2]benzyl alcohol exhibited the presence of a substantial kinetic isotope effect ( kH/kD = 6.20 at 298 K ). This indicated the cleavage of a α-C-H bond in the rate-determining step. An analysis of the temperature dependence of the deuterium isotope effect showed that the loss of hydrogen proceeds through a concerted cyclic process. The rate of oxidation of BA was determined in 19 organic solvents. An analysis of the solvent effect by Swain’s equation indicated that though both the anion and cation-solvating powers of the solvent contribute to the observed solvent effect, the role of cation-solvation is major. The rates of the para and meta compounds, at 298 K, failed to exhibit a significant correlation in terms of Hammett or Brown's substituent constants. The rates were then subjected to analyses in terms of dual substituent parameter (DSP) equations. The rates of oxidation of the para-substituted benzyl alcohols show an excellent correlation with Taft's σI and σRBA values. However, the rates for the meta-substituted benzyl alcohols show an excellent correlation with σI and σR0. The polar reaction constants are negative indicating an electron-deficient transition state. Hence the overall mechanism is proposed to involve the formation of a chromate ester in a fast pre-equilibrium and then a decomposition of the ester in a subsequent slow step via a cyclic concerted symmetrical transition state, involving hydride-ion transfer, leading to the product. The first order dependence on alcohol may be accounted in terms of the small value of the formation constant of the ester intermediate. An another reaction mechanism accounting the acid-catalysis involve the formation of a protonated BIDC prior to formation of an ester intermediate which subsequently decomposes in a slow step leading to the product.Keywords: benzimidazolium dichromate, benzyl alcohols, correlation analysis, kinetics, oxidation
Procedia PDF Downloads 3443664 Remediation of Heavy Metal Contaminated Soil with Vivianite Nanoparticles
Authors: Shinen B., Bavor J., Dorjkhand B., Suvd B., Maitsetseg B.
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A number of remediation techniques are available for the treatment of soils and sediments contaminated by heavy metals. However, some of these techniques are expensive and environmentally disruptive. Nanomaterials are used in the environment as environmental catalysts to convert toxic substances from water, soil, and sediment into environmentally benign compounds. This study was carried out to scrutinize the feasibility of vivianite nanoparticles for remediation of soils contaminated with heavy metals. Column experiments were performed in the laboratory to examine nanoparticle sequestration of metal in soil amended with vivianite nanoparticle suspension. The effect of environmental parameters such as temperature, pH and redox potential on metal leachability and bioavailability of soil amended with nanoparticle suspension was examined and compared with non-amended soils. The vivianite was effective in reducing the leachability of metals in soils. It is suggested that vivianite nanoparticles could be applied for the remediation of contaminated sites polluted by heavy metals due to mining activities, particularly in Mongolia, where mining industries have been developing rapidly in the last decade.Keywords: bioavailability, heavy metals, nanoparticles, remediation
Procedia PDF Downloads 1913663 Molecular Basis of Anti-Biofilm and Anti-Adherence Activity of Syzygium aromaticum on Streptococcus mutans: In Vitro and in Vivo Study
Authors: Mohd Adil, Rosina Khan, Asad U. Khan, Vasantha Rupasinghe HP
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The study examined the effects of Syzygium aromaticum extracts on the virulence properties of Streptococcus mutans. The activity of glucosyltransferases in the presence of crude and diethylether fraction was reduced to 80% at concentration 78.12μg/ml and 39.06μg/ml respectively. The glycolytic pH drop by S. mutans cells was also disrupted by these extracts without affecting the bacterial viability. Microscopic analysis revealed morphological changes of the S. mutans biofilms, indicating that these plant extracts at sub-MICs could significantly affect the ability of S. mutans to form biofilm with distorted extracellular matrix. Furthermore, with the help of quantitative RT-PCR, the expression of different genes involved in adherence, quorum sensing, in the presence of these extracts were down regulated. The crude and active fractions were found effective in preventing caries development in rats. The data showed that S. aromaticum holds promise as a naturally occurring source of compounds that may prevent biofilm-related oral diseases.Keywords: biofilm, quorum sensing, Streptococcus mutans, Syzygium aromaticum extract
Procedia PDF Downloads 3073662 Gesture-Controlled Interface Using Computer Vision and Python
Authors: Vedant Vardhan Rathour, Anant Agrawal
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The project aims to provide a touchless, intuitive interface for human-computer interaction, enabling users to control their computer using hand gestures and voice commands. The system leverages advanced computer vision techniques using the MediaPipe framework and OpenCV to detect and interpret real time hand gestures, transforming them into mouse actions such as clicking, dragging, and scrolling. Additionally, the integration of a voice assistant powered by the Speech Recognition library allows for seamless execution of tasks like web searches, location navigation and gesture control on the system through voice commands.Keywords: gesture recognition, hand tracking, machine learning, convolutional neural networks
Procedia PDF Downloads 123661 Foundations for Global Interactions: The Theoretical Underpinnings of Understanding Others
Authors: Randall E. Osborne
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In a course on International Psychology, 8 theoretical perspectives (Critical Psychology, Liberation Psychology, Post-Modernism, Social Constructivism, Social Identity Theory, Social Reduction Theory, Symbolic Interactionism, and Vygotsky’s Sociocultural Theory) are used as a framework for getting students to understand the concept of and need for Globalization. One of critical psychology's main criticisms of conventional psychology is that it fails to consider or deliberately ignores the way power differences between social classes and groups can impact the mental and physical well-being of individuals or groups of people. Liberation psychology, also known as liberation social psychology or psicología social de la liberación, is an approach to psychological science that aims to understand the psychology of oppressed and impoverished communities by addressing the oppressive sociopolitical structure in which they exist. Postmodernism is largely a reaction to the assumed certainty of scientific, or objective, efforts to explain reality. It stems from a recognition that reality is not simply mirrored in human understanding of it, but rather, is constructed as the mind tries to understand its own particular and personal reality. Lev Vygotsky argued that all cognitive functions originate in, and must therefore be explained as products of social interactions and that learning was not simply the assimilation and accommodation of new knowledge by learners. Social Identity Theory discusses the implications of social identity for human interactions with and assumptions about other people. Social Identification Theory suggests people: (1) categorize—people find it helpful (humans might be perceived as having a need) to place people and objects into categories, (2) identify—people align themselves with groups and gain identity and self-esteem from it, and (3) compare—people compare self to others. Social reductionism argues that all behavior and experiences can be explained simply by the affect of groups on the individual. Symbolic interaction theory focuses attention on the way that people interact through symbols: words, gestures, rules, and roles. Meaning evolves from human their interactions in their environment and with people. Vygotsky’s sociocultural theory of human learning describes learning as a social process and the origination of human intelligence in society or culture. The major theme of Vygotsky’s theoretical framework is that social interaction plays a fundamental role in the development of cognition. This presentation will discuss how these theoretical perspectives are incorporated into a course on International Psychology, a course on the Politics of Hate, and a course on the Psychology of Prejudice, Discrimination and Hate to promote student thinking in a more ‘global’ manner.Keywords: globalization, international psychology, society and culture, teaching interculturally
Procedia PDF Downloads 2523660 Statistical Analysis of the Factors that Influence the Properties of Blueberries from Cultivar Bluecrop
Authors: Raquel P. F. Guiné, Susana R. Matos, Daniela V. T. A. Costa, Fernando J. Gonçalves
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Because blueberries are worldwide recognized as a good source of beneficial components, their consumption has increased in the past decades, and so have the scientific works about their properties. Hence this work was undertaken to evaluate the effect of some production and conservation factors on the properties of blueberries from cultivar Bluecrop. The physical and chemical analyses were done according to established methodologies and then all data was treated using software SPSS for assessment of the possible differences among the factors investigated and/or the correlations between the variables at study. The results showed that location of production influenced some of the berries properties (caliber, sugars, antioxidant activity, color and texture) and that the age of the bushes was correlated with moisture, sugars and acidity, as well as lightness. On the other hand, altitude of the farm only was correlated to sugar content. With regards to conservation, it influenced only anthocyanins content and DPPH antioxidant activity. Finally, the type of extract and the order of extraction had a pronounced influence on all the phnolic properties evaluated.Keywords: Antioxidant activity, blueberry, conservation, geographical origin, phenolic compounds, statistical analysis
Procedia PDF Downloads 4763659 The Effect of the Crystal Field Interaction on the Critical Temperatures and the Sublattice Magnetizations of a Mixedspin-3/2 and Spin-5/2 Ferromagnetic System
Authors: Fathi Abubrig, Mohamed Delfag, Suad Abuzariba
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The influence of the crystal field interactions on the mixed spin-3/2 and spin-5/2 ferromagnetic Ising system is considered by using the mean field theory based on Bogoliubov inequality for the Gibbs free energy. The ground-state phase diagram is constructed, the phase diagrams of the second-order critical temperatures are obtained, and the thermal variation of the sublattice magnetizations is investigated in detail. We find some interesting phenomena for the sublattice magnetizations at particular values of the crystal field interactions.Keywords: crystal field, Ising system, ferromagnetic, magnetization, phase diagrams
Procedia PDF Downloads 4863658 Governance Models of Higher Education Institutions
Authors: Zoran Barac, Maja Martinovic
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Higher Education Institutions (HEIs) are a special kind of organization, with its unique purpose and combination of actors. From the societal point of view, they are central institutions in the society that are involved in the activities of education, research, and innovation. At the same time, their societal function derives complex relationships between involved actors, ranging from students, faculty and administration, business community and corporate partners, government agencies, to the general public. HEIs are also particularly interesting as objects of governance research because of their unique public purpose and combination of stakeholders. Furthermore, they are the special type of institutions from an organizational viewpoint. HEIs are often described as “loosely coupled systems” or “organized anarchies“ that implies the challenging nature of their governance models. Governance models of HEIs describe roles, constellations, and modes of interaction of the involved actors in the process of strategic direction and holistic control of institutions, taking into account each particular context. Many governance models of the HEIs are primarily based on the balance of power among the involved actors. Besides the actors’ power and influence, leadership style and environmental contingency could impact the governance model of an HEI. Analyzing them through the frameworks of institutional and contingency theories, HEI governance models originate as outcomes of their institutional and contingency adaptation. HEIs tend to fit to institutional context comprised of formal and informal institutional rules. By fitting to institutional context, HEIs are converging to each other in terms of their structures, policies, and practices. On the other hand, contingency framework implies that there is no governance model that is suitable for all situations. Consequently, the contingency approach begins with identifying contingency variables that might impact a particular governance model. In order to be effective, the governance model should fit to contingency variables. While the institutional context creates converging forces on HEI governance actors and approaches, contingency variables are the causes of divergence of actors’ behavior and governance models. Finally, an HEI governance model is a balanced adaptation of the HEIs to the institutional context and contingency variables. It also encompasses roles, constellations, and modes of interaction of involved actors influenced by institutional and contingency pressures. Actors’ adaptation to the institutional context brings benefits of legitimacy and resources. On the other hand, the adaptation of the actors’ to the contingency variables brings high performance and effectiveness. HEI governance models outlined and analyzed in this paper are collegial, bureaucratic, entrepreneurial, network, professional, political, anarchical, cybernetic, trustee, stakeholder, and amalgam models.Keywords: governance, governance models, higher education institutions, institutional context, situational context
Procedia PDF Downloads 3363657 Chemical Fingerprinting of the Ephedrine Pathway to Methamphetamine
Authors: Luke Andrighetto, Paul G. Stevenson, Luke C. Henderson, Jim Pearson, Xavier A. Conlan
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As pseudoephedrine, a common ingredient in cold and flu medications is closely monitored and restricted in Australia, alternative methods of accessing it are of interest. The impurities and by-products of every reaction step of pseudoephedrine/ephedrine and methamphetamine synthesis have been mapped in order to develop a chemical fingerprint based on synthetic route. Likewise, seized methamphetamine contains a combination of different cutting agents and starting materials. Therefore, in-silico optimised two-dimensional HPLC with DryLab® and OpenMS® software has been used to efficiently separate complex seizure samples. An excellent match between simulated and real separations was observed. Targeted separation of model compounds was completed with significantly reduced method development time. This study produced a two-dimensional separation regime that offers unprecedented separation power (separation space) while maintaining a rapid analysis time that is faster than those previously reported for gas chromatography, single dimension high performance liquid chromatography or capillary electrophoresis.Keywords: chemical fingerprint, ephedrine, methamphetamine, two-dimensional HPLC
Procedia PDF Downloads 4593656 The Effect of Olea europea L. Extract on Doxorubicin-Induced Cardiotoxicity
Authors: Jessica Maiuolo, Irene Bava, Micaela Gliozzi, Vincenzo Mollace
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Doxorubicin is an anthracycline that is commonly used as a chemotherapy drug due to its cytotoxic effects. The clinical use of doxorubicin is limited due to its known cardiotoxic effects. Polyphenols have a wide range of beneficial properties, and particular importance is given to Oleuropein, one of the main polyphenolic compounds of olive oil. The biological mechanisms involved and the role of the endoplasmic reticulum were examined. Olive oil extract and Oleuropein were able to decrease the damage induced by exposure to doxorubicin. In particular, this natural compound was found to reduce cell mortality and oxidative damage, increase lipid content, and decrease the concentration of calcium ions that escaped from the endoplasmic reticulum. In addition, the direct involvement of this cellular organelle was demonstrated by silencing the ATF6 arm of the Unfolded Protein Response, which was activated after treatment with doxorubicin. The protection afforded by pre-treatment with the natural compound of interest, following the early damage induced by DOXO, provided valuable information regarding the potential use of these substances along with chemotherapy treatment.Keywords: Olea europea L., oleuropein, doxorubicin, endoplasmic reticulum, nutraceutical support
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