Search results for: targeted inhibition

Authors: Madiha El Awamie, Catherine Rees

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Natural preservatives have been used as alternatives to traditional chemical preservatives; however, a limited number have been commercially developed and many remain to be investigated as sources of safer and effective antimicrobials. In this study, we have been investigating the antimicrobial activity of an extract of Glycyrrhiza glabra (liquorice) that was provided as a waste material from the production of liquorice flavourings for the food industry, and to investigate if this retained the expected antimicrobial activity so it could be used as a natural preservative. Antibacterial activity of liquorice extract was screened for evidence of growth inhibition against eight species of Gram-negative and Gram-positive bacteria, including Listeria monocytogenes, Listeria innocua, Staphylococcus aureus, Enterococcus faecalis and Bacillus subtilis. The Gram-negative bacteria tested include Pseudomonas aeruginosa, Escherichia coli and Salmonella typhimurium but none of these were affected by the extract. In contrast, for all of the Gram-positive bacteria tested, growth was inhibited as monitored using optical density. However parallel studies using viable count indicated that the cells were not killed meaning that the extract was bacteriostatic rather than bacteriocidal. The Minimum Inhibitory Concentration [MIC] and Minimum Bactericidal Concentration [MBC] of the extract was also determined and a concentration of 50 µg ml^-1 was found to have a strong bacteriostatic effect on Gram-positive bacteria. Microscopic analysis indicated that there were changes in cell shape suggesting the cell wall was affected. In addition, the use of a reporter strain of Listeria transformed with the bioluminescence genes luxABCDE indicated that cell energy levels were reduced when treated with either 12.5 or 50 µg ml^-1 of the extract, with the reduction in light output being proportional to the concentration of the extract used. Together these results suggest that the extract is inhibiting the growth of Gram-positive bacteria only by damaging the cell wall and/or membrane.

Keywords: antibacterial activity, bioluminescence, Glycyrrhiza glabra, natural preservative

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Authors: Uchenna Egwu, Paul Jonathan Sallis

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Perennial ryegrass is an abundant renewable lignocellulosic biofuel feedstock for biomethane production through anaerobic digestion (AD). In this study, six anaerobic continuously stirred tank reactors (CSTRs) were set up in three pairs. Each pair of the CSTRs was then used to study the effects of operating temperatures – psychrophilic, mesophilic, and thermophilic, and optimum pH on the specific methane production (SMP) of the ryegrass during AD under discontinuous daily feeding conditions. The reactors were fed at an organic loading rate (OLR) ranging from 1-1.5 kgVS.L⁻¹d⁻¹ and hydraulic residence time, HRT=20 days for 140 days. The pH of the digesters was maintained at the range of 6.8-7.2 using 1 M NH₄HCO₃ solution, but this was replaced with biomass ash-extracts from day 105-140. The results obtained showed that the mean SMP of ryegrass measured between HRT 3 and 4 were 318.4, 425.4 and 335 N L CH₄ kg⁻¹VS.d⁻¹ for the psychrophilic (25 ± 2°C), mesophilic (40 ± 1°C) and thermophilic (60 ± 1°C) temperatures respectively. It was also observed that the buffering ability of the reactors increased with operating temperature, probably due to an increase in the solubility of ammonium bicarbonate (NH₄HCO₃) with temperature. The reactors also achieved a mean VS destruction of 61.9, 68.5 and 63.5%, respectively, which signifies that the mesophilic reactors achieved the highest specific methane production (SMP), while the psychrophilic reactors achieved the lowest. None of the reactors attained steady-state condition due to the discontinuous daily feeding times, and therefore, such feeding practice may not be the most effective for maximum biogas production over long periods of time. The addition of NH₄HCO₃ as supplement provided a good buffering condition in these AD digesters, but the digesters failed in the long run due to inhibition from the accumulation of free ammonia, which later led to decrease in pH, acidification, and souring of the digesters. However, the addition of biomass ash extracts was shown to potentially revive failed AD reactors by providing an adequate buffering and essential trace nutrient supplements necessary for optimal bacterial growth.

Keywords: anaerobic digestion, discontinuous feeding, perennial ryegrass, specific methane production, supplements, temperature

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Authors: Protus A. Lumiti, Susan O. Wekesa, Mary Omondi

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Performance is a key pillar to the accomplishment of the goals of all organizations, whether private, public or non- profit. Employees are the intellectual assets of the organization and they are an avenue to the achievement of competitive advantage. An employee welfare service in an organization is vital in fostering employee motivation and improving their productivity. In view of this, the main goal of this research was to determine the relationship between employee welfare practices and the performance of non-governmental organizations in Kenya. The study was guided by four objectives, namely: to establish, determine, evaluate and assess the relationship between employee welfare practices and the performance of non-governmental organizations in Kenya. The study utilized a survey design using both qualitative and quantitative approaches. In this study, a purposive, stratified and simple random sampling technique was used to arrive at a sample of 355 respondents who comprised senior managers, middle level managers and operational employees out of the targeted population of 14,283 employees of non-governmental organizations working in Nairobi County. The primary data collection tools were questionnaires supplemented by an interview schedule, while secondary data was obtained from reviewed journals, published books and articles. Data analysis was done using Statistical Packages for Social Sciences Software version 23. The study utilized multiple linear regression and a structural equation model. The findings of the study were that: employee welfare practices had a positive and significant relationship with the performance of Non-governmental organizations in Kenya. In addition, there was also a linear relationship between the independent variables and the dependent variable and the study concluded that there was a relationship between the predictor variable and the dependent variable of the study. The study recommended that management of No-governmental organization boards in Kenya should come up with a comprehensive policy document on employee welfare practices in order to enhance the performance of non-governmental organizations in Kenya.

Keywords: employee, economic, performance, welfare

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Authors: Arsalan Salahi

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Today, the number of changes in the construction industry and urban mass house building is increasing, which makes you need to pay more attention to targeted planning for human resource management and training. The human resources working in the construction industry have various problems and deficiencies, and in order to solve these problems, there is a need for basic management and training of these people in order to lower the construction costs and increase the quality of the projects, especially in mass house building projects. The success of any project in reaching short and long-term professional goals depends on the efficient combination of work tools, financial resources, raw materials, and most importantly, human resources. Today, due to the complexity and diversity of each project, specialized management fields have emerged to maximize the potential benefits of each component of that project. Human power is known as the most important resource in construction projects for its successful implementation, but unfortunately, due to the low cost of human power compared to other resources, such as materials and machinery, little attention is paid to it. With the correct management and training of human resources, which depends on its correct planning and development, it is possible to improve the performance of construction projects. In this article, the training and motivation of construction industry workers and their effects on the effectiveness of projects in this industry have been researched. In this regard, some barriers to the training and motivation of construction workers and personnel have been identified and solutions have been provided for construction companies. Also, the impact of workers and unskilled people on the efficiency of construction projects is investigated. The results of the above research show that by increasing the use of correct and basic training for human resources, we will see positive results and effects on the performance of construction projects.

Keywords: human resources, construction industry, principled training, skilled and unskilled workers

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Authors: M. Kouyate, M. Sangare, S. Samake, S. Keita, H. G. Kim, D. H. Geschwind

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Background & Objectives: Human genetic studies can be expensive, even unaffordable, in developing countries, partly due to the sequencing costs. Our aim is to pilot the use of bioinformatics tools to guide scientifically valid, locally relevant, and economically sound autism genetic research in Mali. Methods: The following databases, NCBI, HGMD, and LSDB, were used to identify hot point mutations. Phenotype, transmission pattern, theoretical protein expression in the brain, the impact of the mutation on the 3D structure of the protein) were used to prioritize selected autism genes. We used the protein database, Modeller, and clustal W. Results: We found Mef2c (Gly27Ala/Leu38Gln), Pten (Thr131IIle), Prodh (Leu289Met), Nme1 (Ser120Gly), and Dhcr7 (Pro227Thr/Glu224Lys). These mutations were associated with endonucleases BseRI, NspI, PfrJS2IV, BspGI, BsaBI, and SpoDI, respectively. Gly27Ala/Leu38Gln mutations impacted the 3D structure of the Mef2c protein. Mef2c protein sequences across species showed a high percentage of similarity with a highly conserved MADS domain. Discussion: Mef2c, Pten, Prodh, Nme1, and Dhcr 7 gene mutation frequencies in the Malian population will be very informative. PCR coupled with restriction enzyme digestion can be used to screen the targeted gene mutations. Sanger sequencing will be used for confirmation only. This will cut down considerably the sequencing cost for gene-to-gene mutation screening. The knowledge of the 3D structure and potential impact of the mutations on Mef2c protein informed the protein family and altered function (ex. Leu38Gln). Conclusion & Future Work: Bio-informatics will positively impact autism research in Mali. Our approach can be applied to another neuropsychiatric disorder.

Keywords: bioinformatics, endonucleases, autism, Sanger sequencing, point mutations

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Authors: Ferhat Mohamed Amine, Boukhatem Mohamed Nadjib, Chemat Farid

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The Lamiaceae family is widely spread in Algeria. Due to the application of Thymus species growing wild in Algeria as a culinary herb and in folk medicine, the purpose of the present work was to evaluate antimicrobial activities of their essential oils and relate them with their chemical composition, for further application in food and pharmaceutical industries as natural valuable products. The extraction of the Thymus vulgaris L. essential oil (TVEO) was obtained by steam distillation. Chemical composition of the TVEO was determined by Gas Chromatography. A total of thirteen compounds were identified. Carvacrol (83.8%) was the major component, followed by cymene (8.15%) and terpinene (4.96%). Antibacterial action of the TVEO against 23 clinically isolated bacterial strains was determined by using agar disc diffusion and vapour diffusion methods at different doses. By disc diffusion method, TVEO showed potent antimicrobial activity against gram-positive bacteria more than gram-negative strains and antibiotic discs. The Diameter of Inhibition Zone (DIZ) varied from 25 to 60 mm for S. aureus, B. subtilisand E. coli. However, the results obtained by both agar diffusion and vapour diffusion methods were different. Significantly higher antibacterial effect was observed in the vapour phase at lower doses. S. aureus and B. subtilis were the most susceptible strains to the oil vapour. Therefore, smaller doses of EO in the vapour phase can be inhibitory to pathogenic bacteria. There is growing evidence that TVEO in vapour phase are effective antiseptic systems and appears worthy to be considered for practical uses in the treatment of human infections oras air decontaminants in hospital. TVEO has considerable antibacterial activity deserving further investigation for clinical applications. Also whilst the mode of action remains mainly undetermined, this experimental approach will need to continue.

Keywords: antimicrobial drugs, carvacrol, disc diffusion, Thymus vulgaris, vapour diffusion

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Authors: Angel Champion, Sadia Kanwal, Rafat Siddiqui

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Harnessing phytochemicals from plant sources presents a novel opportunity to prevent or treat malignant diseases, including breast cancer. Chemotherapy lacks precision in targeting cancerous cells while sparing normal cells, but a phytopharmaceutical approach may offer a solution. Dandelion, a common weed plant, is rich in phytochemicals and provides a safer, more cost-effective alternative with lower toxicity than traditional pharmaceuticals for conditions such as breast cancer. In this study, an in-vitro experiment will be conducted using the ethanol extract of Dandelion on triple-negative MDA-231 breast cancer cell lines. The polyphenolic analysis revealed that the Dandelion extract, particularly from the root and leaf (both cut and sifted), had the most potent antioxidant properties and exhibited the most potent antioxidation activity from the powdered leaf extract. The extract exhibits prospective promising effects for inducing cell proliferation and apoptosis in breast cancer cells, highlighting its potential for targeted therapeutic interventions. Standardizing methods for Dandelion use is crucial for future clinical applications in cancer treatment. Combining plant-derived compounds with cancer nanotechnology holds the potential for effective strategies in battling malignant diseases. Utilizing liposomes as carriers for phytoconstituent anti-cancer agents offers improved solubility, bioavailability, immunoregulatory effects, advancing anticancer immune function, and reducing toxicity. This integrated approach of natural products and nanotechnology has significant potential to revolutionize healthcare globally, especially in underserved communities where herbal medicine is prevalent.

Keywords: apoptosis, antioxidant activity, cancer nanotechnology, phytopharmaceutical

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Authors: Abdul Rofiq Badril Rizal Muzammil

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Education is an absolute necessity for human’s life that one must fulfill for the entire life. Without education it is impossible for human to develop her/himself well. The education process is an effort to maintain a good behavior within one’s life. Good behavior will be absolutely achieved if it is taught to early-aged children. This paper focuses on how the story telling method enables teachers to make the students have the construction of good behavior and obtain the goal of national education in Indonesia. The targeted students would involve students in As-Solihin kindergarten, Salafiyah-Syafi’iyah Mumbulsari, Jember, Indonesia. Story is what early-aged children like most. Thus, it is a gorgeous chance to make story telling activity as a method to invest Islamic education values to children. This paper, however, also focuses on some deliberately important aspects which of course teachers need to consider including objectives and strategies of the method’s implementation. The teachers will be in need of knowing each student’s characteristic in the classroom so that it would enable them to select appropriate stories that fit best to early aged students. The selected stories are taken from Islamic stories that tell the life of Prophet and heroes of Islam as well as well-known persons in Islam. In addition, there will be a number of activities done in the classroom after the delivery of the story is over on purpose of leading students to have the fundamental foundation of how to build self-awareness in order they could understand better about the importance of being a well-behaved person. After reviewing relevant theories, secondary research and scholars’ opinion involved in all aspects of early-aged children behavior, the author concludes that by leveraging trusted sources, a proactive, co-operative and creative strategy, the teacher can successfully build up children’s good behavior by instilling the Islamic value toward early-aged children through story telling method.

Keywords: story, Islam, children, early age

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Authors: Thilini Kananke

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Culinary herbs have long been considered as significant dietary sources of many potential health-promoting compounds. The present research focused on analysis of antimicrobial, antioxidant and physicochemical properties in selected four culinary herbs namely Murraya koenigii (Curry leaves), Pandanus amaryllifolius (Pandan leaves), Cymbopogon citrates (Lemon grass leaves), and Mentha Piperita (Minchi leaves) obtained from several market sites in Ratnapura District, Sri Lanka. The antimicrobial activity of ethanolic, chloroform and distilled water extracts of culinary herbs were evaluated against the strains of Staphylococcus aureus, Salmonella typhi and Shigella spp. Total phenolic content and the radical scavenging activity (using DPPH assay) of culinary herbs were determined. Four heavy metals (Cu, Cd, Pb and Fe) were analyzed in the selected culinary herbs using the atomic absorption spectroscopy (AAS). Proximate compositions of the selected herbs were analyzed using AOAC official methods. Antimicrobial activity of all selected culinary herbs showed relativity high inhibition zones against S. aureus. Pandan leaves showed the least antimicrobial activity against selected bacterial strains compared with other culinary herbs. Both the highest radical scavenging activity (lower IC50 value) and the total phenolic content (25.57 ±3.54µg GAE/100g) were reported in Mentha piperita extract. The highest concentrations of Cu, Fe and Cd were reported in Curry leaves (29.15 mg/kg), Lemon grass leaves (257.98 mg/kg) and Pandan leaves (6.05 mg/kg) respectively. The heavy metal contents detected in all culinary herbs were below the permitted limits set by WHO/FAO, except Cd. The highest moisture (85.00±0.00%) and fiber (10.66± 2.00%) contents were found in Pandan leaves, while the highest protein (8.94±0.29%), fat (12.3± 2.52%) and ash (3.50± 0.17%) contents were reported in curry leaves. The information obtained from this study highlights the importance of further investigation of other antioxidant, antimicrobial and health promoting compounds of culinary herbs available in Sri Lanka for a detailed comparison.

Keywords: antimicrobial, antioxidant, culinary herbs, proximate analysis

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Authors: Hsi-Chuan Wang, Hongxi Yin

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Compactness has been proposed as a type of sustainable urban form globally. However, the meanings and the measurements might diverse in regarding to the varying interpretation; moreover, since compactness was proposed to eliminate auto culture and urban sprawl in the developed countries, voices have emerged asking to rethink the suitability of compactness in the developing countries – based upon such understanding, Quality of Life (QOL) has been suggested as a good way to show the overall benefit of compactness. In regarding to such background, two subjects were targeted for discussion in this paper: (I) the meaning and feasibility of compactness between the developing and developed countries, and (II) the interaction between compactness and QOL. This paper argues that compactness should not be considered a universal principle for cities of all kind, but rather an ideal concept for urban designer and planner to consider throughout local practices. It firstly reviewed the benefits of both compactness and sprawl to uncover the features behind these urban forms, and later addressed the meaning and difficulty of adopting compactness in both the developing and developed countries. Secondly, arguing compactness to be positioned as a ‘process’ along the transition from the developing countries to the developed ones, this paper applied both cross-sectional and longitudinal analysis to uncover (I) the relationship between compactness and QOL in regarding to 30 American cities and (II) the impact of ‘becoming compact’ on QOL in regarding to 8 identified American Urbanized Areas (UZAs). The findings indicated that higher compactness could link to lower QOL among the compact cities, but with higher QOL among the sprawl cities. In addition, based upon the comparison between 2000 and 2010 on 8 UZAs, their QOL have escalated during the transition from the sprawl areas into the compact ones, but the extent of improvement in QOL could differ greatly among areas. In regarding to our findings, compact development should be proposed as a general guideline leading the contemporary sprawl cities in transition with sustainable urbanism; however, to prevent the externalities from damaging QOL with over-compactness, the compact policy should be flexible to adjust a long-term roadmap for sustainable development.

Keywords: compactness, quality of life, sprawl, sustainable urbanism

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Authors: Laurin Zemmrich, Nicolai Stickler

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With the ongoing debate over how to incorporate sustainability, resilience, and value creation into business strategies, many procurement departments are put under pressure by governments, consumers, non-governmental organizations, and other stakeholders to disclose more information about their supply chains. According to practitioners and experts, procurement benefits the supply chain by increasing transparency and accountability, recruiting new suppliers, and supporting sustainable and ethical sourcing strategies. While most procurement departments establish these objectives, the bulk of activities are not carried out or are not regularly monitored. With the full potential of targeted sourcing still to be realized, procurement executives, in particular, are seeking for short-term cost-cutting impacts to appease external shareholders. We overcome this limitation by using an abductive approach to research and integrating empirical data from a Gioia methodology study design with relevant literature. Our analysis demonstrates that the procurement department has six essential levers aligned with sustainability, resilience, and value creation objectives and contributes to developing a new intra- and interorganizational purpose within the supply chain. Three enablers are identified as having a value-creating effect on supply chain interactions. Additionally, we discovered two impacts that alter the power balance between buyers and suppliers during transactions and have a cost-cutting or cost-avoiding effect. While cost-cutting, cost-avoidance, and dependency-reduction impacts are desirable, redistributing power may also have negative consequences. The article establishes a first strategy framework for evaluating the influence of the procurement department on supply chain transactions, allowing managers to understand better and apply the sourcing function inside a supply chain and embed it throughout the business.

Keywords: supply chain management, resilience, sustainability, value creation, purpose

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Authors: Hongmei Gu, Shaobo Liang, Richard Bergman

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With current worldwide trend in designs to have net-zero emission buildings to mitigate climate change, widespread use of mass timber products, such as Cross Laminated Timber (CLT), or Nail Laminated Timber (NLT) or Dowel Laminated Timber (DLT) in buildings have been proposed as one approach in reducing Greenhouse Gas (GHG) emissions. Consequentially, mass timber building designs are being adopted more and more by architectures in North America, especially for mid- to high-rise buildings where concrete and steel buildings are currently prevalent, but traditional light-frame wood buildings are not. Wood buildings and their associated wood products have tended to have lower environmental impacts than competing energy-intensive materials. It is common practice to conduct life cycle assessments (LCAs) and life cycle cost analyses on buildings with traditional structural materials like concrete and steel in the building design process. Mass timber buildings with lower environmental impacts, especially GHG emissions, can contribute to the Net Zero-emission goal for the world-building sector. However, the economic impacts from CLT mass timber buildings still vary from the life-cycle cost perspective and environmental trade-offs associated with GHG emissions. This paper quantified the Total Life Cycle Cost and cradle-to-grave GHG emissions of a pre-designed CLT mass timber building and compared it to a functionally-equivalent concrete building. The Total life cycle Eco-cost-efficiency is defined in this study and calculated to discuss the trade-offs for the net-zero emission buildings in a holistic view for both environmental and economic impacts. Mass timber used in buildings for the United States is targeted to the materials from the nation’s sustainable managed forest in order to benefit both national and global environments and economies.

Keywords: GHG, economic impact, eco-cost-efficiency, total life-cycle costs

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Authors: Milad Pirali, Sohrab Keyhani, Mohhamad Ali Sanjari, Ali Ashraf Jamshidi

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Purpose: The effect of hamstring antagonist activity on the knee extensors torque of the Anterior Cruciate Ligament reconstruction (ACLR) is not clear and persistent muscle weakness is common after ACLR. Hamstring activation when acting as antagonist is considered very important for knee strengths. Therefore the purpose of this study was to examine hamstring antagonist coactivation during maximal effort of the isokinetic knee extension in ACLR athletes with hamstring autograft. Materials and Methods: We enrolled 20 professional athletes who underwent primary ACLR (hamstring tendon autograft)with 6-24 months postoperative and 20 healthy subjects as control group. Each subjects performed maximal effort isokinetic knee extension and flexion in 60/˚ s and 180/˚ s velocities for the involved and uninvolved limb. Synchronously, surface electromyography (EMG) was recorded of vastus medialis (VM), vastus lateralis (VL), rectus femoris (RF) and biceps femoris (BF). The antagonist integrated EMG (IEMG) values were normalized to the IEMG of the same muscle during maximal isokinetic eccentric effort at the same velocities and ROM. Results: A one-way analysis of variance designs shows significantly greater IEMG coactivation of hamstring and decreased activation of Vm in ACLR when compared to uninvolved and control group leg in 60/˚ s and 180/˚ s velocities. Likewise peak torque to body weight was decreased in ACLR compared to uninvolved and control group during knee extension in both velocities (p < 0.05). Conclusions: Decreased extensors moment caused by decreased quadriceps inhibition and increased hamstring coactivation. In addition, these result indicated to decrease of motor unit recruitment in the VM (as a kinesiologicmonitore of the knee). It is appearing that strengthening of the quadriceps to be an important for rehabilitation program after ACLR for preparation in athletes endeavors. Therefore, we suggest that having more emphasis and focus on quadriceps strength and less emphasis on hamstring following ACLR.

Keywords: ACLR-coactivation, dynamometry, electromyography, isokinetic

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Authors: Erich Ryan, Benjamin McDaniel, Dragoljub Kosanovic

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Combined heat and power (CHP) plants are an efficient technology for meeting the heating and electric needs of large campus energy systems, but have come under greater scrutiny as the world pushes for emissions reductions and lower consumption of fossil fuels. The electrification of heating and cooling systems offers a great deal of potential for carbon savings, but these systems can be costly endeavors due to increased electric consumption and peak demand. Thermal energy storage (TES) has been shown to be an effective means of improving the viability of electrified systems, by shifting heating and cooling load to off-peak hours and reducing peak demand charges. In this study, we analyze the integration of an electrified heating and cooling system with thermal energy storage into a campus CHP plant, to investigate the potential of leveraging existing infrastructure and technologies with the climate goals of the 21st century. A TRNSYS model was built to simulate a ground source heat pump (GSHP) system with TES using measured campus heating and cooling loads. The GSHP with TES system is modeled to follow the parameters of industry standards and sized to provide an optimal balance of capital and operating costs. Using known CHP production information, costs and emissions were investigated for a unique large energy user rate structure that operates a CHP plant. The results highlight the cost and emissions benefits of a targeted integration of heat pump technology within the framework of existing CHP systems, along with the performance impacts and value of TES capability within the combined system.

Keywords: thermal energy storage, combined heat and power, heat pumps, electrification

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Authors: M. Caporale

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French Curricula across the US have recently suffered low enrollment and have experienced difficulties with retention, thus resulting in fewer students minoring and majoring in French and enrolling in upper-level classes. Successful undergraduate programs offer French courses with a strong cultural and interdisciplinary or multidisciplinary component. The World Language Curriculum in liberal arts colleges in America needs to take into account the cultural aspects of the language and encourage students to think critically about the country or countries they are studying. Limiting the critical inquiry to language or literature narrowly defined provides and incomplete and stagnant picture of France and the Francophone world in today's global community. This essay discusses the creation and implementation of a hybrid interdisciplinary L1/L2 course titled "Topics in Francophone Cinema" (subtitle "Francophone Women on Screen and Behind the Camera"). Content-based interdisciplinary courses undoubtedly increase the profile of French and Francophone cultural Studies by introducing students of other disciplines to fundamental questions relating to the French and Francophone cultures (in this case, women's rights in the Francophone world). At the same time, this study determines that through targeted reading and writing assignments, sustained aural exposure to L2 through film,and student participation in a one-credit supplementary weekly practicum (creative film writing workshop), significant advances in L2 competence are achieved with students' oral and written production levels evolving from Advanced Low to Advanced-mid, as defined by the ACFL guidelines. Use of differentiated assessment methods for L1/L2 and student learning outcomes for both groups will also be addressed.

Keywords: interdisciplinary, Francophone cultural studies, language competency, content-based

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Authors: Prem Bahadur Giri, Trilochana Pokhrel

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The nationalization of forest during early 1960s had become a counterproductive for the conservation of forest in Nepal. Realizing this fact, the Government of Nepal initiated a paradigm shift from government-controlled forestry system to people’s direct participation for managing forestry, conceptualizing community forest approach in the early 1980s. The community forestry approach is expected to promote sustainable forest management, restoring degraded forests for enhancing the forest condition on one hand, and on the other, improvement of livelihoods, particularly of low-income people and forest dependent communities, as well as promoting community ownership to forest. As a result, establishment of community forests started and had taken faster momentum in Nepal. Of the total land in Nepal, forest occupies 6.5 million hectares which is around 45 percent of the forest area. Of the total forest area 1.8 million hectarehas been handed-over to community management. A total of 19,361 ‘community forest users groups’ are already created to manage the community forest.Tostreamlinethe governance of community forest, the enactment of ‘Forest Act 1993’ provides a clear legal basis for managing community forest in Nepal. This article is based on an in-depth study taking a case of Tarpakha Community Forest (TCF) located in Siranchok Rural Municipality of Gorkha District in Nepal. It mainly discusses on to extent the TCF able to achieve twin objectives of this community forest for catalyzing socio-economic improvement of the targeted community and conservation of forest. The primary information was generated through in-depth interviews along with group discussion with members, management committee, and other relevant stakeholders. The findings reveal that there is significant improvement of regeneration of forest and also changes in the socio-economic status of local community. However, coordination with local municipality and forest governing entities is still weak.

Keywords: community forest, nepal, socio-economic benefit, sustainable forest management

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Authors: Bushra Zafar, Usman Qamar

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Large data sample size and dimensions render the effectiveness of conventional data mining methodologies. A data mining technique are important tools for collection of knowledgeable information from variety of databases and provides supervised learning in the form of classification to design models to describe vital data classes while structure of the classifier is based on class attribute. Classification efficiency and accuracy are often influenced to great extent by noisy and undesirable features in real application data sets. The inherent natures of data set greatly masks its quality analysis and leave us with quite few practical approaches to use. To our knowledge first time, we present a new approach for investigation of structure and quality of datasets by providing a targeted analysis of localization of noisy and irrelevant features of data sets. Machine learning is based primarily on feature selection as pre-processing step which offers us to select few features from number of features as a subset by reducing the space according to certain evaluation criterion. The primary objective of this study is to trim down the scope of the given data sample by searching a small set of important features which may results into good classification performance. For this purpose, a heuristic for wrapper-based feature selection using genetic algorithm and for discriminative feature selection an external classifier are used. Selection of feature based on its number of occurrence in the chosen chromosomes. Sample dataset has been used to demonstrate proposed idea effectively. A proposed method has improved average accuracy of different datasets is about 95%. Experimental results illustrate that proposed algorithm increases the accuracy of prediction of different diseases.

Keywords: data mining, generic algorithm, KNN algorithms, wrapper based feature selection

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Authors: Husain Rajib, T. H. Sheikh, D. G. Jewel

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Background: Amblyopia is a frequent cause of monocular blindness in children. It can be unilateral or bilateral reduction of best corrected visual acuity associated with decrement in visual processing, accomodation, motility, spatial perception or spatial projection. Anisometropia is an important risk factor for amblyopia that develops when unequal refractive error causes the image to be blurred in the critical developmental period and central inhibition of the visual signal originating from the affected eye associated with significant visual problems including anisokonia, strabismus, and reduced stereopsis. Methods: It is a prospective hospital based study of newly diagnosed of amblyopia seen at the pediatric clinic of Chittagong Eye Infirmary & Training Complex. There were 50 anisometropic amblyopia subjects were examined & questionnaire was piloted. Included were all patients diagnosed with refractive amblyopia between 3 to 13 years, without previous amblyopia treatment, and whose parents were interested to participate in the study. Patients diagnosed with strabismic amblyopia were excluded. Patients were first corrected with the best correction for a month. When the VA in the amblyopic eye did not improve over month, then occlusion treatment was started. Occlusion was done daily for 6-8 hours (full time) together with vision therapy. The occlusion was carried out for 3 months. Results: In this study about 8% subjects had anisometropia from myopia, 18% from hyperopia, 74% from astigmatism. The initial mean visual acuity was 0.74 ± 0.39 Log MAR and after intervention of amblyopia therapy with active vision therapy mean visual acuity was 0.34 ± 0.26 Log MAR. About 94% of subjects were improving at least two lines. The depth of amblyopia associated with type of anisometropic refractive error and magnitude of Anisometropia (p<0.005). By doing this study 10% mild amblyopia, 64% moderate and 26% severe amblyopia were found. Binocular function also decreases with magnitude of Anisometropia. Conclusion: Anisometropic amblyopia is a most important factor in pediatric age group because it can lead to visual impairment. Occlusion therapy with at least one instructed hour of active visual activity practiced out of school hours was effective in anisometropic amblyopes who were diagnosed at the age of 8 years and older, and the patients complied well with the treatment.

Keywords: refractive error, anisometropia, amblyopia, strabismic amblyopia

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Authors: Yu-Wen Cheng, Jau-Der Ho, Liang-Huan Wu, Fan-Li Lin, Li-Huei Chen, Hung-Ming Chang, Yueh-Hsiung Kuo, George Hsiao

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Retina glial activation and neuroinflammation have been confirmed to cause devastating responses in retinodegenerative diseases. The expression and activation of matrix metalloproteinase (MMP)-9 and inducible nitric oxide synthase (iNOS) could be exerted as the crucial pathological factors in glaucoma- and blue light-induced retinal injuries. The present study aimed to investigate the retinoprotective effects and mechanisms of fungal ingredient 3,4-dihydroxybenzalacetone (DBL) isolated from Phellinus linteus in the retinal glial activation and retinodegenerative animal models. According to the cellular studies, DBL significantly and concentration-dependently abrogated MMP-9 activation and expression in TNFα-stimulated retinal Müller (rMC-1) cells. We found the inhibitory activities of DBL were strongly through the STAT- and ERK-dependent pathways. Furthermore, DBL dramatically attenuated MMP-9 activation in the stimulated Müller cells exposed to conditioned media from LPS-stimulated microglia BV-2 cells. On the other hand, DBL strongly suppressed LPS-induced production of NO and ROS and expression of iNOS in microglia BV-2 cells. Consistently, the phosphorylation of STAT was substantially blocked by DBL in LPS-stimulated microglia BV-2 cells. In the evaluation of retinoprotective functions, the high IOP-induced scotopic electroretinographic (ERG) deficit and blue light-induced abnormal pupillary light response (PLR) were assessed. The deficit scotopic ERG responses markedly recovered by DBL in a rat model of glaucoma-like ischemia/reperfusion (I/R)-injury. DBL also reduced the aqueous gelatinolytic activity and retinal MMP-9 expression in high IOP-injured conditions. Additionally, DBL could restore the abnormal PLR and reduce retinal MMP-9 activation. In summary, DBL could ameliorate retinal neuroinflammation and MMP-9 activation by predominantly inhibiting STAT3 activation in the retinal Müller cells and microglia, which exhibits therapeutic potential for glaucoma and other retinal degenerative diseases.

Keywords: glaucoma, blue light, DBL, retinal Müller cell, MMP-9, STAT, Microglia, iNOS, ERG, PLR

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Authors: Tongpong Sriboon, Prapita Thanarak, Chaitawatch Khunrangabsang

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Nowadays, the usage of power generated from photovoltaic system has been promoted significantly in Thailand. The targeted result which is to increase the Solar Power Generation in 2036 to 6000 megawatts (MW) was planned by Alternative Energy Development Plan (AEDP 2015) and Power Development Plan (PDP 2015). The solar rooftop 200 MW was promoted and supported under the Feed-in Tariff scheme (FiT) in two phases; phase I in 2012 and phase II in 2015. However, the number of people interested in supporting the projects reduced due to many reasons which range from the first process to the last that is to sell electricity back to Electricity Authority. This paper will review this situation especially in total electricity generated from solar rooftop system during the day that has been sold back to the grid utility in different capacity FiT rates. With many stakeholders involved, the regulations and criteria were established to maintain the standard of the system. Besides, lots of problems have occurred during the processes including reliability and quality. These problems were shortly followed by other irrevocably issues concerning politics, social, economic etc. In order to effectively develop solar PV power system in Thailand, the problems and solutions were compared to those from six countries including Japan, Australia. America, China, German and Malaysia. This paper particularly focuses on policies and measurement implemented to encourage the rising in solar PV system interest. This review enables one to gain insight into the nature of the changes that have taken place in each and every country mentioned above as well as the underlying reasons behind them. Brief analysis is carried out on identify key challenges and opportunities for solar PV application. This could help create a development path that is suitable with situations to enhance the overall performance of solar PV power generating system in Thailand.

Keywords: solar PV rooftop, PV policy, self-consumption, solar PV power generation

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Authors: Hassan Nour, Nouh Mounadi, Oussama Abchir, Belaidi Salah, Samir Chtita

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Cholinesterase enzymes are biological catalysts essential for the transformation of acetylcholine, which is a neurotransmitter implicated in memory and learning, into acetic acid and choline, altering the neurotransmission process in Alzheimer’s disease patients. Therefore, inhibition of cholinesterase enzymes is a relevant strategy for the symptomatic treatment of Alzheimer’s disease. The current investigation aims to explore potential cholinesterase (ChE) inhibitors through a comprehensive computational approach. Forty-nine phytoconstituents extracted from Cannabis sativa L. were in-silico screened using molecular docking and pharmacokinetic and toxicological analysis to evaluate their possible inhibitory effect on the cholinesterase enzymes. Two phytoconstituents belonging to cannabinoid derivatives were revealed to be promising candidates for Alzheimer's therapy by acting as cholinesterase inhibitors. They have exhibited high binding affinities towards the cholinesterase enzymes and showed their ability to interact with key residues involved in cholinesterase enzymatic activity. In addition, they presented good ADMET profiles allowing them to be promising oral drug candidates. Furthermore, molecular dynamics (MD) simulations were executed to explore their interaction stability under mimetic biological conditions and thus support our findings. To corroborate the docking results, the binding free energy corresponding to the more stable ligand-ChE complexes was re-estimated by applying the MM-PBSA method. MD and MM-PBSA studies affirmed that the ligand-ChE recognition is a spontaneous reaction leading to stable complexes. The conducted investigations have led to great findings that would strongly guide the pharmaceutical industries toward the rational development of potent anti-Alzheimer agents.

Keywords: Alzheimer’s disease, molecular docking, Cannabis sativa L., cholinesterase inhibitors, molecular dynamics, ADMET, MM-PBSA

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Authors: Timothy Scheinert, Eliza Wright

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Background: Link Health is a Boston-based non-profit leveraging in-person and digital platforms to promote health equity. Its primary aim is to financially support low-income individuals through enrollment in federal benefit programs. This study examines the monetary impact of enrollment in several benefit programs. Methodologies: Approximately 17,000 individuals have been screened for eligibility via digital outreach, community events, and in-person clinics. Enrollment and financial distributions are evaluated across programs, including the Affordable Connectivity Program (ACP), Lifeline, LIHEAP, Transitional Aid to Families with Dependent Children (TAFDC), and the Supplemental Nutrition Assistance Program (SNAP). Major Findings: A total of 1,895 individuals have successfully applied, collectively distributing an estimated $1,288,152.00 in aid. The largest contributors to this sum include: ACP: 1,149 enrollments, $413,640 distributed annually. Child Care Financial Assistance (CCFA): 15 enrollments, $240,000 distributed annually. Lifeline: 602 enrollments, $66,822 distributed annually. LIHEAP: 25 enrollments, $48,750 distributed annually. SNAP: 41 enrollments, $123,000 distributed annually. TAFDC: 21 enrollments, $341,760 distributed annually. Conclusions: These results highlight the role of targeted outreach and effective enrollment processes in promoting access to federal benefit programs. High enrollment rates in ACP and Lifeline demonstrate a considerable need for affordable broadband and internet services. Programs like CCFA and TAFDC, despite lower enrollment numbers, provide sizable support per individual. This analysis advocates for continued funding of federal benefit programs. Future efforts can be made to develop screening tools that identify eligibility for multiple programs and reduce the complexity of enrollment.

Keywords: benefits, childcare, connectivity, equity, nutrition

Procedia PDF Downloads 27

Authors: Enlin Lo, Ioannis Dogaris, George Philippidis

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Succinic acid is a compound used for manufacturing lacquers, resins, and other coating chemicals. It is also used in the food and beverage industry as a flavor additive. It is predominantly manufactured from petrochemicals, but it can also be produced by fermentation of sugars from renewable feedstocks, such as plant biomass. Bio-based succinic acid has great potential in becoming a platform chemical (building block) for commodity and high-value chemicals. In this study, the production of bio-based succinic acid from sweet sorghum was investigated. Sweet sorghum has high fermentable sugar content and can be cultivated in a variety of climates. In order to avoid competition with food feedstocks, its non-edible ‘bagasse’ (the fiber part after extracting the juice) was targeted. Initially, various conditions of pretreating sweet sorghum bagasse (SSB) were studied in an effort to remove most of the non-fermentable components and expose the cellulosic fiber containing the fermentable sugars (glucose). Concentrated (83%) phosphoric acid was utilized at temperatures 50-80 oC for 30-60 min at various SSB loadings (10-15%), coupled with enzymatic hydrolysis using commercial cellulase (Ctec2, Novozymes) enzyme, to identify the conditions that lead to the highest glucose yields for subsequent fermentation to succinic acid. As the pretreatment temperature and duration increased, the bagasse color changed from light brown to dark brown-black, indicating decomposition, which ranged from 15% to 72%, while the theoretical glucose yield is 91%. With Minitab software statistical analysis, a model was built to identify the optimal pretreatment condition for maximum glucose released. The projected theoretical bio-based succinic acid production is 23g per 100g of SSB, which will be confirmed with fermentation experiments using the bacterium Actinobacillus succinogenes.

Keywords: biomass, cellulose, enzymatic hydrolysis, fermentation, pretreatment, succinic acid

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Authors: Nusaiba Al-Nemrawi, Belal Al-Husein

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Methotrexate (MTX) is a stoichiometric inhibitor of dihydrofolate reductase, which is essential for DNA synthesis. MTX is a chemotherapeutic agent used for treating many types of cancer cells. However, cells’ resistant to MTX is very common and its pharmacokinetic behavior is highly problematic. of MTX within tumor cells, we propose encapsulation of antitumor drugs in nanoparticulated systems. Chitosan (CS) is a naturally occurring polymer that is biocompatibe, biodegradable, non-toxic, cationic and bioadhesive. CS nanoparticles (CS-NPs) have been used as drug carrier for targeted delivery. Titanium dioxide (TiO2), a natural mineral oxide, which is used in biomaterials due to its high stability and antimicrobial and anticorrosive properties. TiO2 showed a potential as a tumor suppressor. In this study a new formulation of MTX loaded in CS NPs (CS-MTX NPs) and coated with Titanium oxide (TiO2) was prepared. The mean particle size, zeta potential, polydispersity index were measured. The interaction between CS NPs and TiO2 NPs was confirmed using FTIR and XRD. CS-MTX NPs was studied in vitro using the tumor cell line MCF-7 (human breast cancer). The results showed that CS-MTX has a size around 169 nm and as they were coated with TiO2, the size ranged between and depending on the ratio of CS-MTX to TiO2 ratio used in the preparation. All NPs (uncoated and coated carried positive charges and were monodispersed. The entrapment efficacy was around 65%. Both FTIR and XRD proved that TiO2 interacted with CS-MTX NPs. The drug invitro release was controlled and sustained over days. Finally, the studied in vitro using the tumor cell line MCF-7 suggested that combining nanomaterials with anticancer drugs CS-MTX NPs may be more effective than free MTX for cancer treatment. In conclusion, the combination of CS-MTX NPs and TiO2 NPs showed excellent time-dependent in vitro antitumor behavior, therefore, can be employed as a promising anticancer agent to attain efficient results towards MCF-7 cells.

Keywords: Methotrexate, Titanium dioxide, Chitosan nanoparticles, cancer

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Authors: Imad Abdelhamid El-Haci, Wissame Mazari, Fayçal Hassani, Fawzia Atik Bekkara

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Much attention has been paid to the antioxidants, which are expected to prevent food and living systems from peroxidative damage. Incorporation of synthetic antioxidants in food products is under strict regulation due to the potential health hazards caused by such compounds. The use of plants as traditional health remedies is very popular and important for 80% of the world’s population in African, Asian, Latin America and Middle Eastern Countries. Their use is reported to have minimal side effects. In recent years, pharmaceutical companies have spent considerable time and money in developing therapeutics based upon natural products extracted from plants. In other part, due to the continuous emergence of antibiotic-resistant strains there is continual demand for new antibiotics. Chemical compounds from medicinal plant especially are targeted by many researches. In this light, genus Polygonum (Polygonaceae), comprising about 45 genera (300 species), is distributed worldwide, mostly in north temperate regions. They have been reported to have uses in traditional medicine, such as anti-inflammation, promoting blood circulation, dysentery, diuretic, haemorrhage and many other uses. In our study, Polygonum maritimum (from Algerian coast) was extracted with 80% methanol to obtain a crude extract. P. maritimum extract (PME) had a very high content of total phenol, which was 352.49 ± 18.03 mg/g dry weight, expressed as gallic acid equivalent. PME exhibited excellent antioxidant activity, as measured using DPPH and H2O2 scavenging assays. It also showed a high antibacterial activity against gram positive bacterial strains: Bacillus cereus, Bacillus subtilis and Staphylococcus aureus with an MIC 0,12 mg/mL.

Keywords: Polygonum maritimum, crude extract, antioxidant activity, antibacterial activity

Procedia PDF Downloads 311

Authors: Salma E. Ahmed

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Since the mid 50’s, enormous attention has been paid towards nanocarriers and their applications in drug and gene delivery. Among these vesicles, liposomes and micelles have been heavily investigated due to their many advantages over other types. Liposomes, for instance, are mostly distinguished by their ability to encapsulate hydrophobic, hydrophilic and amphiphilic drugs. Micelles, on the other hand, are self-assembled shells of lipids, amphiphilic or oppositely charged block copolymers that, once exposed to aqueous media, can entrap hydrophobic agents, and possess prolonged circulation in the bloodstream. Both carriers are considered compatible and biodegradable. Nevertheless, they have limited stabilities, chemical versatilities, and drug encapsulation efficiencies. In order to overcome these downsides, strategies for optimizing a novel drug delivery system that has the architecture of liposomes and polymeric characteristics of micelles have been evolved. Polymersomes are vehicles with fluidic cores and hydrophobic shells that are protected and isolated from the aqueous media by the hydrated hydrophilic brushes which give the carrier its distinctive polymeric bilayer shape. Similar to liposomes, this merit enables the carrier to encapsulate a wide range of agents, despite their affinities and solubilities in water. Adding to this, the high molecular weight of the amphiphiles that build the body of the polymersomes increases their colloidal and chemical stabilities and reduces the permeability of the polymeric membranes, which makes the vesicles more protective to the encapsulated drug. These carriers can also be modified in ways that make them responsive when targeted or triggered, by manipulating their composition and attaching moieties and conjugates to the body of the carriers. These appealing characteristics, in addition to the ease of synthesis, gave the polymersomes greater potentials in the area of drug delivery. Thus, their design and characterization, in comparison with liposomes and micelles, are briefly reviewed in this work.

Keywords: controlled release, liposomes, micelles, polymersomes, targeting

Procedia PDF Downloads 195

Authors: Hirokatsu Kawashima

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One important element of teaching/learning listening is intensive listening such as listening for precise sounds, words, grammatical, and semantic units. Several classroom-based investigations have been conducted to explore the usefulness of auditory recognition of phonological, grammatical and semantic errors in such a context. The current study reports the results of one such investigation, which targeted auditory recognition of phonological, grammatical, and semantic errors at the sentence level. 56 Japanese EFL learners participated in this investigation, in which their recognition performance of phonological, grammatical and semantic errors was measured on a 9-point scale by learners’ self-evaluation from the perspective of 1) two types of similar English sound (vowel and consonant minimal pair words), 2) two types of sentence word order (verb phrase-based and noun phrase-based word orders), and 3) two types of semantic consistency (verb-purpose and verb-place agreements), respectively, and their general listening proficiency was examined using standardized tests. A number of findings have been made about the interactive relationships between the three types of auditory error recognition and general listening proficiency. Analyses based on the OPLS (Orthogonal Projections to Latent Structure) regression model have disclosed, for example, that the three types of auditory error recognition are linked in a non-linear way: the highest explanatory power for general listening proficiency may be attained when quadratic interactions between auditory recognition of errors related to vowel minimal pair words and that of errors related to noun phrase-based word order are embraced (R2=.33, p=.01).

Keywords: auditory error recognition, intensive listening, interaction, investigation

Procedia PDF Downloads 513

Authors: Nino Chikhladze, Tamar Dochviri, Nato Pitskhelauri, Maia Bitskhinashvili

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Population aging is a key social and demographic trend of the 21st century. Falls represent a prevalent geriatric syndrome that poses significant risks to the health and independence of older adults. The World Health Organization notes a lack of comprehensive data on falls in low- and middle-income countries, complicating the creation of effective prevention programs. To the authors’ best knowledge, no such studies have been conducted in Georgia. The aim of the study is to explore the epidemiology of falls in the elderly population. The hospitalization database of the National Center for Disease Control and Public Health of Georgia was used for the retrospective study. Falls-related injuries were identified using ICD-10 classifications using the class XIX (S and T codes) and class XX for the type of injury (V-Y codes). Statistical data analyses were done using SPSS software version 23.0. The total number of fall-related hospitalizations for individuals aged 65 and older from 2015 to 2021 was 29,697. The study revealed that falls accounted for an average of 63% (ranging from 59% to 66%) of all hospitalizations and 68% (ranging from 65% to 70%) of injury-related hospitalizations during this period. The 69% of all patients were women and 31%-men (Chi2=4482.1, p<0.001). The highest rate of hospitalization was in the age groups 80-84 and 75-79. The probability of fall-related hospitalization was significantly higher in women (p<0.001) compared to men in all age groups except 65-69 years. In the target age group of 65 years and older, the probability of hospitalization increased significantly with an increase in age (p<0.001). The study's results can be leveraged to create evidence-based awareness programs, design targeted multi-domain interventions addressing specific risk factors, and enhance the quality of geriatric healthcare services in Georgia.

Keywords: elderly population, falls, geriatric patients, hospitalization, injuries

Procedia PDF Downloads 28

Authors: Yasser Almazrua

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Terrorism is a multidimensional phenomenon that has increased recently. Many countries started combating terrorism through security forces; however, there has been relatively little attention given to rehabilitation programs for people involved in such terrorism acts. In Saudi Arabia, after facing so many terrorist attacks, they started understanding and countering terrorism differently by establishing Mohammad bin Naif Counselling and Care Center in 2006. The center now is considered one of the top experience centers in the world for terrorist rehabilitation and ideology correction. The center offers different programs such as training, educational, social, art and psychological programs. One of the approaches that have been used by psychological experts at the center is Narrative Therapy. It is a therapeutic approach that focuses on the ability of the client to identify their personal life story. The client during therapy works as a storyteller where he or she gets insight, meaning and better understanding of their own lives. Because each client at the center had a story, it can be better fit method for rehabilitation towards healing and personal development. The case describes a 34-years-old man who was involved in some terrorism activities locally by technically and financially supporting a terrorist group related to Al-Qaida. The beneficiary joined Mohammad bin Naif Counseling and Care Center after serving his sentence. Informed of consent has been given to the beneficiary before starting the therapeutic program. Both qualitative and quantitative data on the beneficiary are collected by self-reporting during the initial session, and by using a psychological measurement. The result found that the beneficiary was not insightful about himself, and he had a high level of repression which relatedly moved him to be targeted for recruitment in the terrorist group. With rehabilitation and by using the therapeutic approach, the beneficiary improved on the level of insight, specifically about himself and also about the experience. This case illustrates the importance of considering the effect of Narrative Therapy in terrorist rehabilitation programs.

Keywords: narrative therapy, rehabilitation, Saudi Arabia, terrorism

Procedia PDF Downloads 296

Authors: Amna J. Ghith, Khaled Abu Zid, Khairia Youssef, Nasser Saad

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Backgrounds: The multikinase and vascular endothelial growth factor (VEGF) receptor inhibitors interrupt the pathway by which angiogenesis becomes established and promulgated, resulting in the inadequate nourishment of metastatic disease. VEGFR-2 has been the principal target of anti-angiogenic therapies. We disclose the new thieno pyrimidines as inhibitors of VEGFR-2 designed by a molecular modeling approach with increased synergistic activity and decreased side effects. Purpose: 2-substituted thieno pyrimidines are designed and synthesized with anticipated anticancer activity based on its in silico molecular docking study that supports the initial pharmacophoric hypothesis with a same binding mode of interaction at the ATP-binding site of VEGFR-2 (PDB 2QU5) with high docking score. Methods: A series of compounds were designed using discovery studio 4.1/CDOCKER with a rational that mimic the pharmacophoric features present in the reported active compounds that targeted VEGFR-2. An in silico ADMET study was also performed to validate the bioavailability of the newly designed compounds. Results: The Compounds to be synthesized showed interaction energy comparable to or within the range of the benzimidazole inhibitor ligand when docked with VEGFR-2. ADMET study showed comparable results most of the compounds showed absorption within (95-99) zone varying according to different substitutions attached to thieno pyrimidine ring system. Conclusions: A series of 2-subsituted thienopyrimidines are to be synthesized with anticipated anticancer activity and according to docking study structure requirement for the design of VEGFR-2 inhibitors which can act as powerful anticancer agents.

Keywords: docking, discovery studio 4.1/CDOCKER, heterocycles based anticancer agents, 2-subsituted thienopyrimidines

Procedia PDF Downloads 246