Search results for: occupational activity

Authors: Vilma Zydziunaite, Gitana Balezentiene, Vilma Zydziunaite

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Teaching is one of most responsible profession, and it is not only a job of an artisan. This profes-sion needs a developed ability to identify oneself with the chosen teaching profession. Research questions: How teachers characterize their authentic individual professional identity? What factors teachers exclude, which support and limit the professional identity? Aim was to develop the grounded theory (GT) about teacher’s professional identity (TPI). Research methodology is based on Charmaz GT version. Data were collected via semi-structured interviews with the he sample of 12 teachers. Findings. 15 extracted categories revealed that the core of TPI is teacher’s professional calling. Premises of TPI are family support, motives for choos-ing teacher’s profession, teacher’s didactic competence. Context of TPI consists of teacher compli-ance with the profession, purposeful preparation for pedagogical studies, professional growth. The strategy of TPI is based on teacher relationship with school community strengthening. The profes-sional frustration limits the TPI. TPI outcome includes teacher recognition, authority; professional mastership, professionalism, professional satisfaction. Dimensions of TPI GT the past (reaching teacher’s profession), present (teacher’s commitment to professional activity) and future (teacher’s profession reconsideration). Conclusions. The substantive GT describes professional identity as complex, changing and life-long process, which develops together with teacher’s personal identity and is connected to professional activity. The professional decision "to be a teacher" is determined by the interaction of internal (professional vocation, personal characteristics, values, self-image, talents, abilities) and external (family, friends, school community, labor market, working condi-tions) factors. The dimensions of the TPI development includes: the past (the pursuit of the teaching profession), the present (the teacher's commitment to professional activity) and the future (the revi-sion of the teaching profession). A significant connection emerged - as the teacher's professional commitment strengthens (creating a self-image, growing the teacher's professional experience, recognition, professionalism, mastery, satisfaction with pedagogical activity), the dimension of re-thinking the teacher's profession weakens. This proves that professional identity occupies an im-portant place in a teacher's life and it affects his professional success and job satisfaction. Teachers singled out the main factors supporting a teacher's professional identity: their own self-image per-ception, professional vocation, positive personal qualities, internal motivation, teacher recognition, confidence in choosing a teaching profession, job satisfaction, professional knowledge, professional growth, good relations with the school community, pleasant experiences, quality education process, excellent student achievements.

Keywords: grounded theory, teacher professional identity, semi-structured interview, school, students, school community, family

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Authors: Benjamin Cramer, Josephine Chau, Helen Little, Erica Randle

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Play Streets provide a safe and open space for children to play and adults to socialize by closing residential streets to through traffic. While research on Play Streets has typically focused on physical activity outcomes in children, there is limited research on the psychosocial health externalities for the wider community. Charles Sturt, a local government area in Adelaide, South Australia, has been hosting Play Streets for several years. The current study is a mixed-methods evaluation of the Charles Sturt Play Streets, concerned with the perceived psychological and social impacts that Play Streets impact on the community. A combination of semi-structured interviews of Play Street organizers and participants will be conducted and analyzed using inductive thematic analysis. Pre-existing survey data will also be analyzed quantitatively and qualitatively to triangulate the findings of the qualitative interviews. The implications of this research are far-reaching, from informing local councils of any additional health benefits of Play Streets, expanding the growing literature on Play Streets beyond childhood physical activity, informing the development of city infrastructure, and advancing the Sustainability Development Goals of Good Health and Wellbeing, Reduced Inequalities, and Sustainable Cities and Communities.

Keywords: play streets, mental health, social health, community health

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Authors: M. Hetmańczyk, R. Polaniak, K. Brukało, E. Grochowska-Niedworok

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Eating behaviours of people are determined by knowledge gained at different stages of life. Children’s diet is especially important. They have to eat meals regularly. Meals should consist of protein, carbohydrates and fat, and drinking the right amount of water. Mistakes in children’s diets affect their health and may lead to health issues such as diabetes, overweight, obesity or malnutrition. The aim of the study was to assess the eating habits among 10-15-year-old children. To achieve this aim, the study included children aged 10-15 years living in Silesia Province, Poland; the participants consisted of 52.08% girls and 47.92% boys. Authorial questionnaire contains 28 questions about eating habits. The results of 192 students were subjected to analysis. The results show that half of the surveyed students participated in physical activity every day. Most children ate 4-5 meals every day, but the breaks between them were too long (four and more hours). Children generally ate cooked meals. Most children ate first breakfast every day, but only one third of studied children ate a second breakfast daily, while 93.75% ate vegetables at least once a day, 94.79% ate fruit at least once a day, and 79.17% drink a daily glass of milk or more. The study found that the eating behaviours of the surveyed children were unsatisfying. While the children did not participate in physical activity often enough, girls took part slightly more often. Children eat second breakfast not often enough. Younger children (10-12 years old) are doing it more often than the older children (13-15 years old). Gender is not a determinant of the frequency of second breakfast consumption.

Keywords: eating habits, children, diet, nutrition status

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Authors: Leila Niroomand, Reza Rafigh

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Nowadays, the world is going under a dramatic change from an industry-centered society to an information-centered one. In other words, we are experiencing a transition from real, physical world into a virtual one. Stepping into the information age and running an effective life within the information-centered society demands getting acquainted with characteristics peculiar to such society. Recently, new technologies such as telecommunication and mobile technologies have changed vehemently and accumulation of achievements and information has become so important and brought about changes in occupational structures. The intellectual structure of this day and age depends on deep attention to creative and knowledge-based human resource collaboration instead of merely functioning human resource. Present study scrutinizes the contribution of different dimensions of mobile technologies including perceived use, perceived enjoyment, continuance intention, confirmation and satisfaction to the creativity of personnel. The statistical population included infrastructure communications company employees totaling 2431 persons out of which 331 individuals were chosen as sample based on Morgan and Krejcie table. This research is descriptive and the questionnaire was used for data gathering and it was distributed among those who used telegram application. 228 questionnaires were analyzed by the researcher. Applying SPSS software, Pierson correlation coefficient was analyzed and it was found out that all dimensions of mobile technologies except satisfaction correlate with the creativity of employees.

Keywords: mobile technologies, continuance intention, perceived enjoyment, confirmation, satisfaction, creativity, perceived use

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Authors: Prakash Singh

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The focus of this paper is on the impact of internal organizational factors on the inappropriate job performance and behaviour of employees. The Buffalo City Metropolitan Municipality (BCMM) in South Africa has been experiencing inappropriate job behaviour and performance of some of its workers. They include misappropriation of resources, maladministration, mismanagement, lack of service delivery, fraud, and corruption. Since many workers in this organization have various levels of formal education, such practices are not expected, because the structural-functionalist assumption is that formal education is a solution to societal challenges. Since inappropriate job behaviour and performance continue to be reported in spite of the formal education of BCMM workers, this study seeks to investigate how the two phenomena co-exist. It thus seeks to put into perspective the paradoxical co-existence of formal education with inappropriate job behaviour and performance, by focusing on the BCMM as a case-study. For data collection, this study used the mixed method approach; that is, a combination of qualitative and quantitative methods. The findings revealed structural, systemic and human impediments to labour productivity in the organization. By and large, the unquestioning acceptance of the assumption that the skills shortage is responsible for inappropriate workers’ job performance and behaviour is discredited by the evidence of skilled personnel who exercise their responsibilities in a manner that undermines their occupational requirements. Therefore, this exploratory study affirms that the narrow conception of skills, that privileges job-specific capabilities, is not enough for cultivating a workforce with appropriate job behaviour and performance practices.

Keywords: inappropriate job behaviour, labour productivity, mismanagement, skills shortage

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Authors: Rahimah Abdulrahman, A. Eardle, Wilfred Alan, Abdel Hamid Soliman

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With the rapid development in technology, and advances in learning technologies, m-learning has begun to occupy a great part of our lives. The pace of the life getting together with the need for learning started mobile learning (m-learning) concept. In 2008, Saudi Arabia requested a national plan for the adoption of information technology (IT) across the country. Part of the recommendations of this plan concerns the implementation of mobile learning (m-learning) as well as their prospective applications to higher education within the Kingdom of Saudi Arabia. The overall aim of the research is to explore the main issues that impact the deployment of m-learning in nursing institutes in Saudi Arabia, at the Armed Force Hospitals (AFH), Alhada. This is in order to be able to develop a generic model to enable and assist the educational policy makers and implementers of m-learning, to comprehend and treat those issues effectively. Specifically, the research will explore the concept of m-learning; identify and analyse the main organisational; technological and cultural issue, that relate to the adoption of m-learning; develop a model of m-learning; investigate the perception of the students of the Nursing Institutes to the use of m-learning technologies for their nursing diploma programmes based on their experiences; conduct a validation of the m-learning model with the use of the nursing Institute of the AFH, Alhada in Saudi Arabia, and evaluate the research project as a learning experience and as a contribution to the body of knowledge. Activity Theory (AT) will be adopted for the study due to the fact that it provides a conceptual framework that engenders an understanding of the structure, development and the context of computer-supported activities. The study will be adopt a set of data collection methods which engage nursing students in a quantitative survey, while nurse teachers are engaged through in depth qualitative studies to get first-hand information about the organisational, technological and cultural issues that impact on the deployment of m-learning. The original contribution will be a model for developing m-learning material for classroom-based learning in the nursing institute that can have a general application.

Keywords: activity theory (at), mobile learning (m-learning), nursing institute, Saudi Arabia (sa)

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Authors: Mario Gómez, Won Ho Kim, Ángel Licona, José Carlos Rodríguez

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This article analyzes innovation activity in Mexico and South Korea. It develops an econometric model to test for structural breaks in the number of patent applications filed by residents and nonresidents in these countries during the period of 1965 to 2012. These changes may suggest that firms’ innovative capabilities have changed because of implementing different science, technology and innovation (STI) policies in Mexico and South Korea. Two important features characterize this research from others already developed by these authors. First, the theoretical research framework in this research is the debate between the assimilation view of growth and the accumulation view of growth. This characteristic suggests that trade liberalization should be accompanied by an adequate STI policy to boost competitiveness among indigenous firms. Second, the analysis in this research stresses the importance of key actors (e.g. governments) to successfully develop innovation capabilities among indigenous firms. Therefore, the question conducting this research is how STI policies in Mexico and South Korea contributed to develop firms’ innovation capabilities in these countries during last decades? The results from this research suggests that STI policy in South Korea was more suitable to boost innovation firms to compete in markets. Data to develop this research was released by the World Intellectual Property Organization (WIPO).

Keywords: innovation, Mexico, South Korea, science, technology and innovation policy

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Authors: Osama H. Elsayed, Mohsen M. S. Asker, Mahmoud A. Swelim, Ibrahim H. Abbas, Aziza I. Attwa, Mohamed E. El Awady

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Hydroxy marilone C is a bioactive metabolite was produced from the culture broth of Streptomyces badius isolated from Egyptian soil. hydroxy marilone C was purified and fractionated by silica gel column with a gradient mobile phase dicloromethane (DCM) : Methanol then Sephadex LH-20 column using methanol as a mobile phase. It was subjected to many instruments as Infrared (IR), nuclear magnetic resonance (NMR), Mass spectroscopy (MS) and UV spectroscopy to the elucidation of its structure. It was evaluated for antioxidant, cytotoxicity against human alveolar basal epithelial cell line (A-549) and human breast adenocarcinoma cell line (MCF-7) and antiviral activities; showed that the maximum antioxidant activity was 78.8 % at 3000 µg/ml after 90 min. and the IC50 value against DPPH radical found about 1500 µg/ml after 60 min. By Using MTT assay the effect of the pure compound on the proliferation of A-549 cells and MCF-7 cells were 443 µg/ml and 147.9 µg/ml, respectively. While for detection of antiviral activity using Madin-Darby canine kidney (MDCK) cells the maximum cytotoxicity was at 27.9% and IC50 was 128.1µg/ml. The maximum concentration required for protecting 50% of the virus-infected cells against H1N1 viral cytopathogenicity (EC50) was 33.25% for 80 µg/ml. This results indicated that the hydroxy marilone C has a potential antitumor and antiviral activities.

Keywords: hydroxy marilone C, production, bioactive compound, Streptomyces badius

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Authors: Mercy Vivian Sulaiman, Pablo Chavajay

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This study examined parents ways of supporting and facilitating their first-grade children in a book-activity in Nigeria and the United States. Seventy-five parent-child dyads (38 from Nigeria and 37 from the U.S.) were video recorded constructing narratives around a wordless picture book. Analyses focused on identifying parents’ means of facilitating children’s involvement as well as parents and children's reliance on questions and statements during the shared activity. Nigerian parents assumed a sole narrator approach, guiding the narratives and providing most of the information to their children through referential questions and referential and behavioral statements. Unlike the Nigerian parents, US parents engaged in a shared narrator approach, encouraging and building more on their children's contributions, asking more inferential and yes/no questions, and making more inferential and yes/no statements. Nigerian and US children’s extent and types of questions and statements made during their involvement in the activities varied and their contributions resembled those of their parents in their respective cultural groups. These findings highlight significant cultural variations and similarities in book-sharing practices between parents and children, underscoring the role of parental approaches to children's narrative construction and their impact on their learning.

Keywords: book-sharing, cultural differences, parent-child interactions, narrative contributions, Nigeria, united states

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Authors: Catarina Bento, Ana Carolina Gonçalves, Fábio Jesus, Luís Rodrigues Silva

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Increasing evidence suggests that a diet rich in fruits and vegetables plays important roles in the prevention of chronic diseases, such as heart disease, cancer, stroke, diabetes, Alzheimer’s disease, among others. Fruits and vegetables gained prominence due their richness in bioactive compounds, being the focus of many studies due to their biological properties acting as health promoters. Prunus avium Linnaeus (L.), commonly known as sweet cherry has been the centre of attention due to its health benefits, and has been highly studied. In Portugal, most of the cherry production comes from the Fundão region. The Saco is one of the most important cultivar produced in this region, attributed with geographical protection. In this work, we prepared 3 extracts through solid-phase extraction (SPE): a whole extract, fraction I (non-coloured phenolics) and fraction II (coloured phenolics). The three extracts were used to determine the phenolic profile of Saco cultivar by liquid chromatography with diode array detection (LC-DAD) technique. This was followed by the evaluation of their biological potential, testing the extracts’ capacity to scavenge free-radicals (DPPH•, nitric oxide (•NO) and superoxide radical (O2●-)) and to inhibit α-glucosidase enzyme of all extracts. Additionally, we evaluated, for the first time, the protective effects against peroxyl radical (ROO•)-induced hemoglobin oxidation and hemolysis in human erythrocytes. A total of 16 non-coloured phenolics were detected, 3-O-caffeoylquinic and ρ-coumaroylquinic acids were the main ones, and 6 anthocyanins were found, among which cyanidin-3-O-rutinoside represented the majority. In respect to antioxidant activity, Saco showed great antioxidant potential in a concentration-dependent manner, demonstrated through the DPPH•,•NO and O2●-radicals, and greater ability to inhibit the α-glucosidase enzyme in comparison to the regular drug acarbose used to treat diabetes. Additionally, Saco proved to be effective to protect erythrocytes against oxidative damage in a concentration-dependent manner against hemoglobin oxidation and hemolysis. Our work demonstrated that Saco cultivar is an excellent source of phenolic compounds which are natural antioxidants that easily capture reactive species, such as ROO• before they can attack the erythrocytes’ membrane. In a general way, the whole extract showed the best efficiency, most likely due to a synergetic interaction between the different compounds. Finally, comparing the two separate fractions, the coloured fraction showed the most activity in all the assays, proving to be the biggest contributor of Saco cherries’ biological activity.

Keywords: biological potential, coloured phenolics, non-coloured phenolics, sweet cherry

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Authors: Mehrdad Arabi, Ehsan Beheshtitabar, Bahador Ghadirifaraz, Behrooz Forjanizadeh

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Interaction between human, location and activity defines space. In the framework of these relations, space is a container for current specifications in relations of the 3 mentioned elements. The change of land utility considered with average performance range, urban regulations, society requirements etc. will provide welfare and comfort for citizens. From an engineering view it is fundamental that choosing a proper location for a specific civil activity requires evaluation of locations from different perspectives. The debate of desirable establishment of municipal service elements in urban regions is one of the most important issues related to urban planning. In this paper, the research type is applicable based on goal, and is descriptive and analytical based on nature. Initially existing terminals in Esfahan are surveyed and then new locations are presented based on evaluated criteria. In order to evaluate terminals based on the considered factors, an AHP model is used at first to estimate weight of different factors and then existing and suggested locations are evaluated using Arc GIS software and AHP model results. The results show that existing bus terminals are located in fairly proper locations. Further results of this study suggest new locations to establish terminals based on urban criteria.

Keywords: Arc GIS, Esfahan city, optimum locations, terminals

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Authors: Kaustuvmani Patowary, Suresh Deka

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Oil pollution accidents, nowadays, have become a common phenomenon and have caused ecological and social disasters. Microorganisms with high oil-degrading performance are essential for bioremediation of petroleum hydrocarbon. In this investigation, an effective biosurfactant producer and hydrocarbon degrading bacterial strain, Pseudomonas sp.PG1 (identified by 16s rDNA sequencing) was isolated from hydrocarbon contaminated garage soil of Pathsala, Assam, India, using crude oil enrichment technique. The growth parameters such as pH and temperature were optimized for the strain and upto 81.8% degradation of total petroleum hydrocarbon (TPH) has been achieved after 5 weeks when grown in mineral salt media (MSM) containing 2% (w/v) crude oil as the carbon source. The biosurfactant production during the course of hydrocarbon degradation was monitored by surface tension measurement and emulsification activity. The produced biosurfactant had the ability to decrease the surface tension of MSM from 72 mN/m to 29.6 mN/m, with the critical micelle concentration (CMC)of 56 mg/L. The biosurfactant exhibited 100% emulsification activity on crude oil. FTIR spectroscopy and LCMS-MS analysis of the purified biosurfactant revealed that the biosurfactant is Rhamnolipidic in nature with several rhamnolipid congeners. Gas Chromatography-Mass spectroscopy (GC-MS) analysis clearly demonstrated that the strain PG1 efficiently degrade different hydrocarbon fractions of the crude oil. The study suggeststhat application of the biosurfactant producing strain PG1 as an appropriate candidate for bioremediation of crude oil contaminants.

Keywords: petroleum hydrocarbon, hydrocarbon contamination, bioremediation, biosurfactant, rhamnolipid

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Authors: Esther Acha, Jose Cambra, De Chen

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Hydrogen is considered an important energy vector for the 21st century. Nowadays there are some difficulties for hydrogen economy implantation, and one of them is the high purity required for hydrogen. This energy vector is still being mainly produced from fuels, from wich hydrogen is produced as a component of a mixture containing other gases, such as CO, CO2 and H2O. A forthcoming sustainable pathway for hydrogen is steam-reforming of bio-oils derived from biomass, e.g. via fast pyrolysis. Bio-oils are a mixture of acids, alcohols, aldehydes, esters, ketones, sugars phenols, guaiacols, syringols, furans, multi-functional compounds and also up to a 30 wt% of water. The sorption enhanced steam reforming (SESR) process is attracting a great deal of attention due to the fact that it combines both hydrogen production and CO2 separation. In the SESR process, carbon dioxide is captured by an in situ sorbent, which shifts the reversible reforming and water gas shift reactions to the product side, beyond their conventional thermodynamic limits, giving rise to a higher hydrogen production and lower cost. The hydrogen containing mixture has been obtained from the SESR of bio-oil type compounds. Different types of catalysts have been tested. All of them contain Ni at around a 30 wt %. Two samples have been prepared with the wet impregnation technique over conventional (gamma alumina) and non-conventional (olivine) supports. And a third catalysts has been prepared over a hydrotalcite-like material (HT). The employed sorbent is a commercial dolomite. The activity tests were performed in a bench-scale plant (PID Eng&Tech), using a stainless steel fixed bed reactor. The catalysts were reduced in situ in the reactor, before the activity tests. The effluent stream was cooled down, thus condensed liquid was collected and weighed, and the gas phase was analysed online by a microGC. The hydrogen yield, and process behavior was analysed without the sorbent (the traditional SR where a second purification step will be needed but that operates in steady state) and the SESR (where the purification step could be avoided but that operates in batch state). The influence of the support type and preparation method will be observed in the produced hydrogen yield. Additionally, the stability of the catalysts is critical, due to the fact that in SESR process sorption-desorption steps are required. The produced hydrogen yield and hydrogen purity has to be high and also stable, even after several sorption-desorption cycles. The prepared catalysts were characterized employing different techniques to determine the physicochemical properties of the fresh-reduced and used (after the activity tests) materials. The characterization results, together with the activity results show the influence of the catalysts preparation method, calcination temperature, or can even explain the observed yield and conversion.

Keywords: CO2 sorbent, enhanced steam reforming, hydrogen

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Authors: Dileep Maarisetty, Janaki Komandur, Saroj S. Baral

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In the current work, photocatalytic degradation of phenol was carried both in UV and visible light to find the slowest step that is limiting the rate of photo-degradation process. Characterization such as XRD, SEM, FT-IR, TEM, XPS, UV-DRS, PL, BET, UPS, ESR and zeta potential experiments were conducted to assess the credibility of catalysts in boosting the photocatalytic activity. To explore the synergy, TiO₂ was doped with graphene and alumina. The orbital hybridization with alumina doping (mediated by graphene) resulted in higher electron transfer from the conduction band of TiO₂ to alumina surface where oxygen reduction reactions (ORR) occur. Besides, the doping of alumina and graphene introduced defects into Ti lattice and helped in improving the adsorptive properties of modified photo-catalyst. Results showed that these defects promoted the oxygen reduction reactions (ORR) on the catalyst’s surface. ORR activity aims at producing reactive oxygen species (ROS). These ROS species oxidizes the phenol molecules which is adsorbed on the surface of photo-catalysts, thereby driving the photocatalytic reactions. Since mass transfer is considered as rate limiting step, various mathematical models were applied to the experimental data to probe the best fit. By varying the parameters, it was found that intra-particle diffusion was the slowest step in the degradation process. Lagergren model gave the best R² values indicating the nature of rate kinetics. Similarly, different adsorption isotherms were employed and realized that Langmuir isotherm suits the best with tremendous increase in uptake capacity (mg/g) of TiO₂-rGO-Al₂O₃ as compared undoped TiO₂. This further assisted in higher adsorption of phenol molecules. The results obtained from experimental, kinetic modelling and adsorption isotherms; it is concluded that apart from changes in surface, optoelectronic and morphological properties that enhanced the photocatalytic activity, the intra-particle diffusion within the catalyst’s pores serve as rate-limiting step in deciding the fate of photo-catalytic degradation of phenol.

Keywords: ORR, phenol degradation, photo-catalyst, rate kinetics

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Authors: Abubakar Salisu Garba

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The objective of the paper is to highlight the nature of entrepreneurial activities in the Sub Sahara Africa. Five countries in the Sub Sahara African that are participating in Global Entrepreneurship Monitor (GEM) research have been studied to understand the types of entrepreneurial activities and their socio-economic implications in the region. The importance of entrepreneurial activities in boosting socio-economic development has been recognized not only in developing countries, but across the entire global economies. Some people believe that the wealth and poverty of developing countries is associated with nature and type of entrepreneurial activity. Policy makers are not only concern about the rate of business start up, but the growth and development of those starts up is of paramount importance to the development of the country’s economy. Although, the supply of entrepreneurs is essential, sometimes it does not really matters in boosting economic performance. What is more important is having high impact entrepreneurs who could make meaningful contribution to the economy. High growth oriented entrepreneurs are more stable and contribute greatly in enhancing the economic performance. When entrepreneurs are facing difficulties in sustaining and growing their businesses, it may be unlikely for entrepreneurship to reduce unemployment and poverty. Inadequate financial supports, insufficient infrastructure, lack of enforcing laws protecting the right of entrepreneurs are some of the problems making business environment difficult in Sub-Saharan Africa.

Keywords: entrepreneurship, entrepreneurial activity, job creation, poverty reduction, Sub-Saharan Africa

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Authors: Xinyu Wei, Mingming Peng, Kenji Kamiya, Eika Qian

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Iso-stearic acid as a saturated fatty acid with a branched chain shows a low pour point, high oxidative stability and great biodegradability. The industrial production of iso-stearic acid involves first isomerizing unsaturated fatty acids into branched-chain unsaturated fatty acids (BUFAs), followed by hydrogenating the branched-chain unsaturated fatty acids to obtain iso-stearic acid. However, the production yield of iso-stearic acid is reportedly less than 30%. In recent decades, extensive research has been conducted on branched fatty acids. Most research has replaced acidic clays with zeolites due to their high selectivity, good thermal stability, and renewability. It was reported that isomerization of unsaturated fatty acid occurred mainly inside the zeolite channel. In contrast, the production of by-products like dimer acid mainly occurs at acid sites outside the surface of zeolite. Further, the deactivation of catalysts is attributed to the pore blockage of zeolite. In the present study, micro/mesoporous ZSM-22 zeolites were developed. It is clear that the synthesis of a micro/mesoporous ZSM-22 zeolite is regarded as the ideal strategy owing to its ability to minimize coke formation. Different mesoporosities micro/mesoporous H-ZSM-22 zeolites were prepared through recrystallization of ZSM-22 using sodium hydroxide solution (0.2-1M) with cetyltrimethylammonium bromide template (CTAB). The structure, morphology, porosity, acidity, and isomerization performance of the prepared catalysts were characterized and evaluated. The dissolution and recrystallization process of the H-ZSM-22 microporous zeolite led to the formation of approximately 4 nm-sized mesoporous channels on the outer surface of the microporous zeolite, resulting in a micro/mesoporous material. This process increased the weak Brønsted acid sites at the pore mouth while reducing the total number of acid sites in ZSM-22. Finally, an activity test was conducted using oleic acid as a model compound in a fixed-bed reactor. The activity test results revealed that micro/mesoporous H-ZSM-22 zeolites exhibited a high isomerization activity, reaching >70% selectivity and >50% yield of BUFAs. Furthermore, the yield of oligomers was limited to less than 20%. This demonstrates that the presence of mesopores in ZSM-22 enhances contact between the feedstock and the active sites within the catalyst, thereby increasing catalyst activity. Additionally, a portion of the dissolved and recrystallized silica adhered to the catalyst's surface, covering the surface-active sites, which reduced the formation of oligomers. This study offers distinct insights into the production of iso-stearic acid using a fixed-bed reactor, paving the way for future research in this area.

Keywords: Iso-stearic acid, oleic acid, skeletal isomerization, micro/mesoporous, ZSM-22

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Authors: M. Muneer, Waseem Raza

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Nano-crystalline materials of pure and metal-doped semiconducting materials have been successfully synthesized using sol gel and hydrothermal methods. The prepared materials were characterized by standard analytical techniques, i.e., XRD, SEM, EDX, UV–vis Spectroscopy and FTIR. The (XRD) analysis showed that the obtained particles are present in partial crystalline nature and exhibit no other impurity phase. The EDX and (SEM) images depicted that metals have been successfully loaded on the surface of the semiconductor. FTIR showed an additional absorption band at 910 cm−1, characteristic of absorption band indicating the incorporation of dopant into the lattice in addition to a broad and strong absorption band in the region of 410–580 cm−1 due to metal–O stretching. The UV–vis absorption spectra of synthesized particles indicate that the doping of metals into the lattice shift the absorption band towards the visible region. Thermal analysis, measurement of the synthesized sample showed that the thermal stability of pure semiconducting material is decreased due to increase in dopant concentration. The photocatalytic activity of the synthesized particles was studied by measuring the change in concentration of three different chromophoric dyes as a function of irradiation time. The photocatalytic activity of doped materials were found to increase with increase in dopant concentration.

Keywords: photocatalysis, metal doped semicondcutors, dye degradation, visible light active materials

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Authors: Min Liu, Jirui Gong, Qinpu Luo, Lili Yang, Bo Yang, Zihe Zhang, Yan Pan, Zhanwei Zhai

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Grazing disturbance is one of the important land-use types that affect plant growth and ecosystem processes. In order to study the responses of dominant species to grazing in the semiarid temperate grassland of Inner Mongolia, we set five grazing intensity plots: a control and four levels of grazing (light (LG), moderate (MG), heavy (HG) and extreme heavy grazing (EHG)) to test the morphological and physiological responses of Stipa grandis, Leymus chinensis at the individual levels. With the increase of grazing intensity, Stipa grandis and Leymus chinensis both exhibited reduced plant height, leaf area, stem length and aboveground biomass, showing a significant dwarf phenomenon especially in HG and EHG plots. The photosynthetic capacity decreased along the grazing gradient. Especially in the MG plot, the two dominant species have lowest net photosynthetic rate (Pn) and water use efficiency (WUE). However, in the HG and EHG plots, the two species had high light saturation point (LSP) and low light compensation point (LCP), indicating they have high light-use efficiency. They showed a stimulation of compensatory photosynthesis to the remnant leaves as compared with grasses in MG plot. For Leymus chinensis, the lipid peroxidation level did not increase with the low malondialdehyde (MDA) content even in the EHG plot. It may be due to the high enzymes activity of superoxide dismutase (SOD) and peroxidase (POD) to reduce the damage of reactive oxygen species. Meanwhile, more carbohydrate was stored in the leaf of Leymus chinensis to provide energy to the plant regrowth. On the contrary, Stipa grandis showed the high level of lipid peroxidation especially in the HG and EHG plots with decreased antioxidant enzymes activity. The soluble protein content did not change significantly in the different plots. Therefore, with the increase of grazing intensity, plants changed morphological and physiological traits to defend themselves effectively to herbivores. Leymus chinensis is more resistant to grazing than Stipa grandis in terms of tolerance traits, particularly under heavy grazing pressure.

Keywords: antioxidant enzymes activity, grazing density, morphological responses, photosynthesis

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Authors: Mohamed Moussaoui, Mouna Baassi, Soukayna Baammi, Hatim Soufi, Mohammed Salah, Rachid Daoud, Achraf EL Allali, Mohammed Elalaoui Belghiti, Said Belaaouad

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The present study aims to investigate the quantitative structure-activity relationship (QSAR) of a series of Thiazole derivatives reported as anticancer agents (hepatocellular carcinoma), using principally the electronic descriptors calculated by the density functional theory (DFT) method and by applying the multiple linear regression method. The developed model showed good statistical parameters (R²= 0.725, R²ₐ𝒹ⱼ= 0.653, MSE = 0.060, R²ₜₑₛₜ= 0.827, Q²𝒸ᵥ = 0.536). The energy of the highest occupied molecular orbital (EHOMO) orbital, electronic energy (TE), shape coefficient (I), number of rotatable bonds (NROT), and index of refraction (n) were revealed to be the main descriptors influencing the anti-cancer activity. Additional Thiazole derivatives were then designed and their activities and pharmacokinetic properties were predicted using the validated QSAR model. These designed molecules underwent evaluation through molecular docking (MD) and molecular dynamic (MD) simulations, with binding affinity calculated using the MMPBSA script according to a 100 ns simulation trajectory. This process aimed to study both their affinity and stability towards Cyclin-Dependent Kinase 2 (CDK2), a target protein for cancer disease treatment. The research concluded by identifying four CDK2 inhibitors - A1, A3, A5, and A6 - displaying satisfactory pharmacokinetic properties. MDs results indicated that the designed compound A5 remained stable in the active center of the CDK2 protein, suggesting its potential as an effective inhibitor for the treatment of hepatocellular carcinoma. The findings of this study could contribute significantly to the development of effective CDK2 inhibitors.

Keywords: QSAR, ADMET, Thiazole, anticancer, molecular docking, molecular dynamic simulations, MMPBSA calculation

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Authors: Jyoti Singh, Ranju Bansal

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Fighting pain and inflammation is a common problem faced by physicians while dealing with a wide variety of diseases. Since ancient time nonsteroidal anti-inflammatory agents (NSAIDs) and opioids have been the cornerstone of treatment therapy, however, the usefulness of both these classes is limited due to severe side effects. NSAIDs, which are mainly used to treat mild to moderate inflammatory pain, induce gastric irritation and nephrotoxicity whereas opioids show an array of adverse reactions such as respiratory depression, sedation, and constipation. Moreover, repeated administration of these drugs induces tolerance to the analgesic effects and physical dependence. Further discovery of selective COX-2 inhibitors (coxibs) suggested safety without any ulcerogenic side effects; however, long-term use of these drugs resulted in kidney and hepatic toxicity along with an increased risk of secondary cardiovascular effects. The basic approaches towards inflammation and pain treatment are constantly changing, and researchers are continuously trying to develop safer and effective anti-inflammatory drug candidates for the treatment of different inflammatory conditions such as osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, psoriasis and multiple sclerosis. Synthetic 3(2H)-pyridazinones constitute an important scaffold for drug discovery. Structure-activity relationship studies on pyridazinones have shown that attachment of a lactam at N-2 of the pyridazinone ring through a methylene spacer results in significantly increased anti-inflammatory and analgesic properties of the derivatives. Further introduction of the heterocyclic ring at lactam nitrogen results in improvement of biological activities. Keeping in mind these SAR studies, a new series of compounds were synthesized as shown in scheme 1 and investigated for anti-inflammatory, analgesic, anti-platelet activities and docking studies. The structures of newly synthesized compounds have been established by various spectroscopic techniques. All the synthesized pyridazinone derivatives exhibited potent anti-inflammatory and analgesic activity. Homoveratryl substituted derivative was found to possess highest anti-inflammatory and analgesic activity displaying 73.60 % inhibition of edema at 40 mg/kg with no ulcerogenic activity when compared to standard drugs indomethacin. Moreover, 2-substituted-4-benzo[d][1,3]dioxole-6-phenylpyridazin-3(2H)-ones derivatives did not produce significant changes in bleeding time and emerged as safe agents. Molecular docking studies also illustrated good binding interactions at the active site of the cyclooxygenase-2 (hCox-2) enzyme.

Keywords: anti-inflammatory, analgesic, pyridazin-3(2H)-one, selective COX-2 inhibitors

Procedia PDF Downloads 200

Authors: Muhammad Ali Khan

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Education is a word has been derived from Latin word "Educare", means to train. Therefore, the harmonious growth of the potentialities for achieving the qualities desirable and useful in the human society is called education. It is claimed that by educating women we can develop our economy, family health and decrease population growth. To explore the socio-economic impact of education on urban women. A prospective study design was used. Over a period of six months 50 respondents were randomly selected from Hayat Abad, an urban city in the North West of Pakistan. A questionnaire was used to explore marital, educational, occupational, social, economical and political status of urban women. Of the total, 50% (25) were employed, where 56% were married and 44% unmarried. Of the employed participants, 56% were teachers fallowed by social worker 16%. Monthly income was significantly high (p=001) of women with master degree. Understanding between wife and husband was also very significant in women with masters. . 78% of employed women replied that Parda (Hija) should be on choice not imposed. 52% of educated women replied participation in social activates, such as parties, shopping etc. Education has a high impact on urban women because it is directly related to employment, decision of power, economy and social life. Urban women with high education have significant political awareness and empowerment. Improving women educational level in rural areas of Pakistan is the key for economic growth and political empowerment

Keywords: women, urban, Pakistan, socio economic

Procedia PDF Downloads 102

Authors: E. Kilicay, Z. Karahaliloglu, B. Hazer, E. B. Denkbas

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In this study, we have prepared concanavaline A (ConA) functionalized curcumin (CUR) loaded PHBHHx (poly(3-hydroxybutyrate-co-3-hydroxyhexanoate)) nanoparticles as a novel and efficient drug delivery system. CUR is a promising anticancer agent for various cancer types. The aim of this study was to evaluate therapeutic potential of curcumin loaded PHBHHx nanoparticles (CUR-NPs) and concanavaline A conjugated curcumin loaded NPs (ConA-CUR NPs) for ovarian cancer treatment. ConA was covalently connected to the carboxylic group of nanoparticles by EDC/NHS activation method. In the ligand attachment experiment, the binding capacity of ConA on the surface of NPs was found about 90%. Scanning electron microscopy (SEM) and atomic force microscopy (AFM) analysis showed that the prepared nanoparticles were smooth and spherical in shape. The size and zeta potential of prepared NPs were about 228±5 nm and −21.3 mV respectively. ConA-CUR NPs were characterized by FT-IR spectroscopy which confirmed the existence of CUR and ConA in the nanoparticles. The entrapment and loading efficiencies of different polymer/drug weight ratios, 1/0.125 PHBHHx/CUR= 1.25CUR-NPs; 1/0.25 PHBHHx/CUR= 2.5CUR-NPs; 1/0.5 PHBHHx/CUR= 5CUR-NPs, ConA-1.25CUR NPs, ConA-2.5CUR NPs and ConA-5CUR NPs were found to be ≈ 68%-16.8%; 55%-17.7 %; 45%-33.6%; 70%-15.7%; 60%-17%; 51%-30.2% respectively. In vitro drug release showed that the sustained release of curcumin was observed from CUR-NPs and ConA-CUR NPs over a period of 19 days. After binding of ConA, the release rate was slightly increased due to the migration of curcumin to the surface of the nanoparticles and the matrix integrities was decreased because of the conjugation reaction. This functionalized nanoparticles demonstrated high drug loading capacity, sustained drug release profile, and high and long term anticancer efficacy in human cancer cell lines. Anticancer activity of ConA-CUR NPs was proved by MTT assay and reconfirmed by apoptosis and necrosis assay. The anticancer activity of ConA-CUR NPs was measured in ovarian cancer cells (SKOV-3) and the results revealed that the ConA-CUR NPs had better tumor cells decline activity than free curcumin. The nacked nanoparticles have no cytotoxicity against human ovarian carcinoma cells. Thus the developed functionalized nanoformulation could be a promising candidate in cancer therapy.

Keywords: curcumin, curcumin-PHBHHx nanoparticles, concanavalin A, concanavalin A-curcumin PHBHHx nanoparticles, PHBHHx nanoparticles, ovarian cancer cell

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Authors: Raviv Harris, Maggie Levy

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Natural product-based pesticides may serve as an alternative to the traditional synthetic pesticides, which have a potentially damaging effect, both to human health and for the environment. Along with plants, microorganisms are a prospective source of such biological pesticides. A unique and active strain of P. aphidis (designated isolate L12, Israel 2004), an epiphytic and non-pathogenic basidiomycete yeast, was isolated in our lab from strawberry leaves. P. aphidis L12 secretions were found to inhibit broad range of plant pathogens. This work demonstrates that metabolites isolated from the biocontrol agent P. aphidis (isolate L12) can inhibit varied fungal and bacterial phytopathogens. Biologically active metabolites were extracted from P. aphidis biomass, using the organic solvent ethyl acetate. The antimicrobial activity of the extract was demonstrated, both in vitro and in planta. Using disk diffusion assays, the following inhibition zones were obtained: 43cm² for Pseudomonas syringae pv. tomato, 28.5cm² for Xanthomonas campestris pv. vesicatoria, 59cm² for Clavibacter michiganensis subsp. michiganensis, 34cm² for Erwinia amylovora and 34cm² for Agrobacterium tumefaciens. Additionally, strong inhibitory activity of the extract against fungi mycelial growth was established, with IC₅₀ values of 606µg ml⁻¹ for Botrytis cinerea, 221µg ml⁻¹ for Pythium spp., 519µg ml⁻¹ for Rhizoctonia solani, 455µg ml⁻¹ for Sclerotinia sclerotiorum, 2270µg ml⁻¹ for Fusarium oxysporum f. sp. lycopersici, and 2038µg ml⁻¹ for Alternaria alternata. The results of the in planta experiments demonstrated a dose-dependent reduction in disease infection. Significant inhibition of B. cinerea lesions on tomato plants was obtained when a spore suspension of this pathogen was treated with extract concentrations higher than 4.2mg ml⁻¹. Concentration of 7mg ml⁻¹ caused a reduction of over 95% in the lesion size of B. cinerea on tomato plants. The strong antimicrobial activity demonstrated both in vitro and in planta against varied phytopathogens, may indicate that the extracted antimicrobial metabolites have potential to serve as natural pesticides in the field.

Keywords: antimicrobial, B. cinerea, metabolites, natural pesticides, P. aphidis

Procedia PDF Downloads 231

Authors: Rozelle Labuschagne, Ronel Roos

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Individuals often experience a reduction in physical function, quality of life and basic activities of daily living after surgery. This is exponentially true for high-risk patients, especially the elderly and frail individuals. Not much is known about the physical function, physical activity preferences and factors associated with the six-minute walk test of elderly individuals who would undergo elective abdominal surgery in South Africa. Such information is important to design effective prehabilitation physiotherapy programs prior to elective surgery. The purpose of the study was to describe the demographic profile and physical function of elderly patients who would undergo elective surgery and to determine factors associated with their six-minute walk test distance findings. A cross-sectional descriptive study in elderly patients older than 60 years of age who would undergo elective abdominal surgery were consecutively sampled at a private hospital in Pretoria, South Africa. Participants’ demographics were collected and physical function assessed with the Functional Comorbidity Index (FCI), DeMorton Mobility Index (DEMMI), Lawton-Brody Instrumental Activities of Daily Living Scale (IADL) and six-minute walk test (6MWT). Descriptive and inferential statistics were used for data analysis with IBM SPSS 25. A p-value ≤ 0.05 were deemed statistically significant. The pilot study consisted of 12 participants (female (n=11, 91.7%), male (n=1, 8.3%) with a mean age of 65.8 (±4.5) years, body mass index of 28 (±4.2) kg.m2 with one (8.3%) participant being a current smoker and four (33.3%) participants having a smoking history. Nine (75%) participants lived independently at home and three (25%) had caregivers. Participants reported walking (n=6, 50%), stretching exercises (n=1, 8.3%), household chores & gardening (n=2, 16.7%), biking/swimming/running (n=1, 8.3%) as physical activity preferences. Physical function findings of the sample were: mean FCI score 3 (±1.1), DEMMI score 81.1 (±14.9), IADL 95 (±17.3), 6MWT 435.50 (IQR 364.75-458.50) with percentage 6MWT distance achieved 81.8% (IQR 64.4%-87.5%). A strong negative correlation was observed between 6MWT distance walked and FCI (r = -0.729, p=0.007). The majority of study participants reported incorporating some form of physical activity into their daily life as form of exercise. Most participants did not achieve their predicted 6MWT distance indicating less than optimal levels of physical function capacity. The number of comorbidities as determined by the FCI was associated with the distance that participants could walk with the 6MWT. The results of this pilot study could be used to indicate which elderly individuals would benefit most from a pre-surgical rehabilitation program. The main goal of such a program would be to improve physical function capacity as measured by the 6MWT. Surgeons could refer patients based on age and number of comorbidities, as determined by the FCI, to potentially improve surgical outcomes.

Keywords: abdominal surgery, elderly, physical function, six-minute walk test

Procedia PDF Downloads 197

Authors: Nawel Boucherba, Azzedine Bettache, Abdelaziz Messis, Francis Duchiron, Said Benallaoua

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The impetus for research in the field of bioseparation has been sparked by the difficulty and complexity in the downstream processing of biological products. Indeed, 50% to 90% of the production cost for a typical biological product resides in the purification strategy. There is a need for efficient and economical large scale bioseparation techniques which will achieve high purity and high recovery while maintaining the biological activity of the molecule. One such purification technique which meets these criteria involves the partitioning of biomolecules between two immiscible phases in an aqueous system (ATPS). The Production of xylanases is carried out in 500ml of a liquid medium based on birchwood xylan. In each ATPS, PEG 1000 is added to a mixture consisting of dipotassium phosphate, sodium chloride and the culture medium inoculated with the strain Jonesia denitrificans, the mixture was adjusted to different pH. The concentration of PEG 1000 was varied: 8 to 16 % and the NaCl percentages are also varied from 2 to 4% while maintaining the other parameters constant. The results showed that the best ATPS for purification of xylanases is composed of PEG 1000 at 8.33%, 13.14 % of K2HPO4, 1.62% NaCl at pH 7. We obtained a yield of 96.62 %, a partition coefficient of 86.66 and a purification factor of 2.9. The zymogram showed that the activity is mainly detected in the top phase.

Keywords: Jonesia denitrificans BN13, xylanase, aqueous two phases system, zymogram

Procedia PDF Downloads 399

Authors: Kang-Hyun Leem, Myung-Gyou Kim, Hye Kyung Kim

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Velvet antler (VA), the immature antlers of male deer, is traditionally used for thousands of years in Asian countries, such as Korea, China, Taiwan, and Mongolia. It has been considered to improve immune system and physical strength. The goal of this study was to investigate the immunomodulatory effect of deer antler velvet using in vitro system. In the first step, the effects of VA (70% ethanol extract) on the proliferation of splenocytes, bone marrow cell, and macrophages were determined. Next, the effect of VA on the production of nitric oxide and phagocytic activity in macrophage were measured. The results showed that VA treatment increased concanavalin-A stimulated splenocyte, bone marrow cells, and macrophage proliferation in a dose dependent manner. VA at 50 and 100 ug/mL concentrations significantly enhanced the concanavalin-A stimulated splenocyte proliferation by 8.8% and 18.5%, respectively. The proliferation of bone marrow cells, isolated from 5wk-old ICR mice, were increased by 25.2% and 46.5% by 50 and 100 ug/mL VA treatment. RAW 264.7 cell proliferation reached peak value at 50 ug/mL of VA treatment exhibiting 108% of the basal value. Nitric oxide production by RAW 264.7 macrophage cells was slightly reduced by VA treatment but was not statistically significant. Moreover, the phagocytic activity of macrophages was enhanced by VA treatment. These results indicate that VA is effective in immune system.

Keywords: deer antler, splenocyte, bone marrow cells, macrophage proliferation, phagocytosis

Procedia PDF Downloads 272

Authors: Andrii Shalaginov, Katrin Franke, Xiongwei Huang

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One of the leading problems in Cyber Security today is the emergence of targeted attacks conducted by adversaries with access to sophisticated tools. These attacks usually steal senior level employee system privileges, in order to gain unauthorized access to confidential knowledge and valuable intellectual property. Malware used for initial compromise of the systems are sophisticated and may target zero-day vulnerabilities. In this work we utilize common behaviour of malware called ”beacon”, which implies that infected hosts communicate to Command and Control servers at regular intervals that have relatively small time variations. By analysing such beacon activity through passive network monitoring, it is possible to detect potential malware infections. So, we focus on time gaps as indicators of possible C2 activity in targeted enterprise networks. We represent DNS log files as a graph, whose vertices are destination domains and edges are timestamps. Then by using four periodicity detection algorithms for each pair of internal-external communications, we check timestamp sequences to identify the beacon activities. Finally, based on the graph structure, we infer the existence of other infected hosts and malicious domains enrolled in the attack activities.

Keywords: malware detection, network security, targeted attack, computational intelligence

Procedia PDF Downloads 264

Authors: Zohreh Hajiha

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Culture affects the ability of the organization in expressing and achieving the goals. Organizational culture influences the selection of instruments applied in the management of organizations. All the instruments applied in organizations to control, promote and create innovations are influenced by organizational culture. This research studies organizational culture based on the cultural model of Muijen and its relationship with applying management accounting innovations in Iranian listed firms. Management accounting innovations of this study include activity-based costing, activity-based management, balanced scorecard, target costing, standard costing, quality costing, Kaizen costing and dimensions of organizational culture include support orientation, innovation orientation, rules orientation and goal orientation. 105 questionnaires were sent to financial executives of production companies and 73 questionnaires were returned. The findings show that there is a significant difference between organizational culture of firms that have applied management accounting innovations and those which have used these innovations less. Also, dimensions of support orientation and culture goal orientation are the highest in groups that apply management accounting innovations. The findings suggest that proper organization culture could promote the use od management accounting tools in Iranian firms.

Keywords: organizational culture, innovation, management accounting, muijen model

Procedia PDF Downloads 360

Authors: Samy Selim

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Natural products are still major sources of innovative therapeutic agents for various conditions, including infectious diseases. Peganum harmala L. oil had wide range uses as traditional medicinal plants. The current study was designed to evaluate the antibacterial activity of P. harmala essential oil. The chemical constitutes and toxicity of these oils was also determined to obtain further information on the correlation between the chemical contents and antibacterial activity. The antibacterial effect of the essential oils of P. harmala oil was studied against some foodborne pathogenic bacteria species. The oil of plant was subjected to gas chromatography-mass spectrometry (GC/MS). The impact of oils administration on the change in rate of weight gain and complete blood picture in hamsters were investigated. P. harmala oil had strong antibacterial effect against bacterial species especially at minimum inhibitory concentration (MIC) less than 75.0 μg/ml. From the oil of P. harmala, forty one compounds were identified, and the major constituent was 1-hexyl-2-nitrocyclohexane (9.07%). Acute toxicity test was performed on hamsters and showed complete survival after 14 days, and there were no toxicity symptoms occurred. This study demonstrated that these essential oils seemed to be destitute of toxic effect which could compromise the medicinal use of these plants in folk medicine.

Keywords: analysis mass spectrometry, antibacterial activities, acute toxicity, chemical constitutes, gas chromatography, weight gain, Peganum harmala

Procedia PDF Downloads 486

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 95