Search results for: bloodstream expression site

Authors: Muhammad Habib, Lin Tang, Guoliang Xue, Attaur Rahman, Myong-Ho Kim, Soonil Lee, Xuefan Zhou, Yan Zhang, Dou Zhang

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Designing a high-performance, lead-free ceramic has become a cutting-edge research topic due to growing concerns about the toxic nature of lead-based materials. In this work, a convenient strategy of compositional design and domain engineering is applied to the lead-fee BiFeO₃-BaTiO₃ ceramics, which provides a flexible polarization-free-energy profile for domain switching. Here, simultaneously enhanced dynamic piezoelectric constant (d33* = 772 pm/V) and a good thermal-stability (d33* = 26% over the temperature of 20-180 ᵒC) are achieved with a high Curie temperature (TC) of 432 ᵒC. This high piezoelectric strain performance is collectively attributed to multiple effects such as thermal quenching, suppression of defect charges by donor doping, chemically induced local structure heterogeneity, and electric field-induced phase transition. Furthermore, the addition of BT content decreased octahedral tilting, reduced anisotropy for domain switching and increased tetragonality (cₜ/aₜ), providing a wider polar length for B-site cation displacement, leading to high piezoelectric strain performance. Atomic-resolution transmission electron microscopy and piezoelectric force microscopy combined with X-ray diffraction results strongly support the origin of high piezoelectricity. The high and temperature-stable piezoelectric strain response of this work is superior to those of other lead-free ceramics. The synergistic approach of composition design and the concept present here for the origin of high strain response provides a paradigm for the development of materials for high-temperature piezoelectric actuator applications.

Keywords: Piezoelectric, BiFeO3-BaTiO3, Quenching, Temperature-insensitive

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Authors: Hadjer Messabih

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The M’zab architecture has preserved its identity that was able to endure for centuries conserving practically the same way of life and the same building techniques since the 11th century. Even more, the newly built ksar Tafilelt is also designed to meet the local tradition. In 1996, a community led project was initiated to build a “new ksar” named Tafilelt based on a traditional form of community-led cooperative housing. It is a unique experience in the field of community housing that reproduces traditional architectural patterns while addressing contemporary ways of life with their expected modern comfort. This research is based on the hypothesis that the process of producing ksar Tafilelt is culturally responsive to a conservative community that was characterized by certain values which were transmitted to this ksar manifesting as cultural continuity. It aims at investigating what type of cultural continuity manifests itself in the co-production of ksar Tafilelt and the way the settlement and its houses are produced and inhabited, as well as the new emerging values and adaptive transition in social relations. The research methodology is based on a combination of questionnaires, in depth interviews, photography, and site visit to record and demonstrate how these buildings respond to peoples’ needs. Post Occupancy Evaluation (POE) is also employed in order to understand the lessons that can be learned from this project. Finally, this study proves that the cultural continuity that was transmitted from the Ibadi community is sill manifested in ksar Tafilelt, which provided strong religious bonds and a strong sense of community. The research findings have resulted in a number of lessons and principles that can be learnt from the project of ksar Tafilelt which can inform future practices of housing provision and design in Algeria and other countries.

Keywords: community-led cooperative housing, conservative community, cultural continuity, post occupancy evaluation

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Authors: Penina Orenstein

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In today’s world, particularly with COVID-19 a constant worldwide threat, organizations need greater visibility over their supply chains more than ever before, in order to find areas for improvement and greater efficiency, reduce the chances of disruption and stay competitive. The concept of supply chain mapping is one where every process and route is mapped in detail between each vendor and supplier. The simplest method of mapping involves sourcing publicly available data including news and financial information concerning relationships between suppliers. An additional layer of information would be disclosed by large, direct suppliers about their production and logistics sites. While this method has the advantage of not requiring any input from suppliers, it also doesn’t allow for much transparency beyond the first supplier tier and may generate irrelevant data—noise—that must be filtered out to find the actionable data. The primary goal of this research is to build data maps of supply chains by focusing on a layered approach. Using these maps, the secondary goal is to address the question as to whether the supply chain is re-engineered to make improvements, for example, to lower the carbon footprint. Using a drill-down approach, the end result is a comprehensive map detailing the linkages between tier-one, tier-two, and tier-three suppliers super-imposed on a geographical map. The driving force behind this idea is to be able to trace individual parts to the exact site where they’re manufactured. In this way, companies can ensure sustainability practices from the production of raw materials through the finished goods. The approach allows companies to identify and anticipate vulnerabilities in their supply chain. It unlocks predictive analytics capabilities and enables them to act proactively. The research is particularly compelling because it unites network science theory with empirical data and presents the results in a visual, intuitive manner.

Keywords: data mining, supply chain, empirical research, data mapping

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Authors: Seyyed Mohammad Amin Mousavi Sagharchi, Elham Javanroudi

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Introduction: Tuberculosis (TB) is a known disease with hidden features caused by Mycobacterium tuberculosis (MTB). This disease, which is one of the 10 deadliest in the world, has caused millions of deaths in recent decades. Furthermore, TB is responsible for infecting about 30% population of world. Like any infection, TB can activate the immune system by locating and colonization in the human body, especially in the alveoli. TB is granulomatosis, so MTB can absorb the host’s immune cells and other cells to form granuloma. Method: Different databases (e.g., PubMed) were recruited to prepare this paper and fulfill our goals to search and find effective papers and investigations. Results: Immune response to MTB is related to T cell killers and contains CD1, CD4, and CD8 T lymphocytes. CD1 lymphocytes can recognize glycolipids, which highly exist in the Mycobacterial fatty cell wall. CD4 lymphocytes and macrophages form granuloma, and it is the main line of immune response to Mycobacteria. On the other hand, CD8 cells have cytolytic function for directly killing MTB by secretion of granulysin. Other functions and secretion to the deal are interleukin-12 (IL-12) by induction of expression interferon-γ (INF-γ) for macrophages activation and creating a granuloma, and tumor necrosis factor (TNF) by promoting macrophage phagolysosomal fusion. Conclusion: Immune cells in battle with MTB are macrophages, dendritic cells (DCs), neutrophils, and natural killer (NK) cells. These immune cells can recognize the Mycobacterium by various receptors, including Toll-like receptors (TLRs), Nod-like receptors (NLRs), and C-type lectin receptors (CLRs) located in the cell surface. In human alveoli exist about 50 dendritic macrophages, which have close communication with other immune cells in the circulating system and epithelial cells to deal with Mycobacteria. Against immune cells, MTB handles some factors (e.g., cordfactor, O-Ag, lipoarabinomannan, sulfatides, and adenylate cyclase) and practical functions (e.g., inhibition of macrophages).

Keywords: mycobacterium tuberculosis, immune responses, immunological mechanisms, respiratory tuberculosis

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Authors: Rafooneh Mokhtarshahi Sani

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This study explores how the residents of a conserved urban area have used goods and ideas as resources to maintain an enviable architectural identity. Whereas conserved urban quarters are seen as role model for maintaining architectural identity, the article describes how their residents try to give a contemporary modern image to their homes. It is argued that despite the efforts of authorities and decision makers to keep and preserve the traditional architectural identity in conserved urban areas, people have already moved on and have adjusted their homes with their preferred architectural taste. Being through such conflict of interests, have put the future of architectural identity in such places at risk. The thesis is that, on the one hand, such struggle over a desirable symbolic status in identity formation is taking place, and, on the other, it is continuously widening the gap between the real and ideal identity in the built environment. The study then analytically connects the concept of symbolic status to current identity debates. As an empirical research, this study uses systematic social and physical observation methods to describe and categorize the characteristics of settlements in Walled City of Famagusta, which symbolically represent the modern houses. The Walled City is a cultural heritage site, which most of its urban context has been conserved. Traditional houses in this area demonstrate the identity of North Cyprus architecture. The conserved residential buildings, however, either has been abandoned or went through changes by their users to present the ideal image of contemporary life. In the concluding section, the article discusses the differences between the symbolic status of people and authorities in defining a culturally valuable contemporary home. And raises the question of whether we can talk at all about architectural identity in terms of conserving the traditional style, and how we may do so on the basis of dynamic nature of identity and the necessity of its acceptance by the users.

Keywords: symbolic status, architectural identity, conservation, facades, Famagusta walled city

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Authors: Eric Sitorus, Septian Prahastudhi, Turgod Nainggolan, Erwin Riyanto

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Mining by block or panel caving is a mining method that takes advantage of fractures within an ore body, coupled with gravity, to extract material from a predetermined column of ore. The caving column is weakened from beneath through the use of undercutting, after which the ore breaks up and is extracted from below in a continuous cycle. The nature of this method induces cyclical stresses on the pillars of excavations as stress is built up and released over time, which has a detrimental effect on both the installed ground support and the rock mass itself. Ground support capacity, especially on the production where excavation void ratio is highest, is subjected to heavy loading. Strain above threshold of the elongation of support capacity can yield resulting in damage to excavations. Geotechnical engineers must evaluate not only the remnant capacity of ground support systems but also investigate depth of rock mass yield within pillars, backs and floors. Ground Penetrating Radar (GPR) is a geophysical method that has the ability to evaluate rock mass damage using electromagnetic waves. This paper illustrates a case study from the Grasberg mining complex where non-invasive information on the depth of damage and condition of the remaining rock mass was required. GPR with 100 MHz antenna resolution was used to obtain images of the subsurface to determine rehabilitation requirements prior to recommencing production activities. The GPR surveys were used to calibrate the reflection coefficient response of varying rock mass conditions to known Rock Quality Designation (RQD) parameters observed at the mine. The calibrated GPR survey allowed site engineers to map subsurface conditions and plan rehabilitation accordingly.

Keywords: block caving, ground penetrating radar, reflectivity, RQD

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Authors: Joohyun Park, Jin Baek

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The purpose of this study is to Analyze the role and effect arise from Diagonal Plane Control by Street Width (DPCSW) in Architecture in Seoul, and to predict the aspect of transition about the relationship among buildings and Urban morphology After the abolition. To find the tendency of building shape regulation, This study review Building Acts concerned with form making (the building to land Ratio, building designated line, wall designated line, building height limit (DPCSW) and etc.) and simulate the shape of urban blocks made by Acts in drawings. The review results show DPCSW is not only limitation about height, but also making the building setback from road and make the Road broader. And it makes the typical shape of the urban block that buildings are moving away from surrounding road After the Abolition of DPCSW; it is expected by the legislature that domestic real estate’s market would be promoted by increased total floor areas in each building. Some substitution from the legislature is announced, but it just deals with Building Maximum unit by Block unit except the regulation about arrangement in urban Figure and Ground. In conclusion, refrain from the uncontrolled development of city, It is important to make regulation about not only height factors but limitation line in land. Furthermore, through revising District Unit Plan, It is positively necessary to reset the relationship between buildings for the making the city space better.

Keywords: diagonal plane control by street width, building maximum height, district unit plan, building acts, urban block type, morphology, building shape

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Authors: Dharshika Rajalingam, Jeffery W. Peng

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Acinetobacter baumannii is a challenging threat to global health, recognized as a multidrug-resistant pathogen. -lactamase is one of the principal resistant mechanisms developed by A. baumannii to survive against -lactam antibiotics. OXA24/40 is one of the types of -lactamases, a well-documented carbapenem hydrolyzing class D -lactamases (CHDL). It was revealed that OXA24/40 showed resistivity against doripenem, one of the carbapenems, by two different mechanisms as hydrolysis and -lactonization. Furthermore, it undergoes genetic mutations to broaden the -lactamase activity to survive against antibiotic environments. One of the crucial characterizations of prokaryotes to develop adaptation is post-translational modification (PTM), mainly phosphorylation. However, the PTM of OXA24/40 is an unknown feature, and the impact of PTM on antibiotic resistivity is yet to be explored. We approached these hypotheses using NMR and MS techniques and found that the OXA24/40 could be phosphorylated in vitro. The Ser81 at the active STFK motif of OXA24/40 of catalytic pocket was identified as the site of phosphorylation using 1D 31P NMR experiment, whereas S81 is required to form an acyl-enzyme complex between enzyme and -lactam antibiotics. The activity of completely phosphorylated OXA24/40 wild type against doripenem revealed that the phosphorylation of active Ser inactivates the -lactamases activity of OXA24/40. The 1D 1H CPMG NMR-based activity assay of phosphorylated OXA24/40 against doripenem confirmed that both deactivating mechanisms are inhibited by phosphorylation. Carbamylated Lysine at the active STFK motif is one of the critical features of CHDL required for the acylation and deacylation reactions of the enzyme. The 1D 13C NMR experiment confirmed that the K84 of phosphorylated OXA24/40 is de-carbamylated. Phosphorylation of OXA24/40 affects both active S81 and carbamylated K84 of OXA24 that are required for the resistivity of -lactamase. So, phosphorylation could be one of the reasons for the genetic mutation of OXA24/40 for the development of antibiotic resistivity. Further research can lead to an understanding of the effect of phosphorylation on the clinical mutants of the OXA24-like -lactamase family on the broadening of -lactamase activity.

Keywords: OXA24/40, phosphorylation, clinical mutants, resistivity

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Authors: Leticia Leandro Rade, Amanda Silva de Sousa, Suman Das, Wesley Generoso, Mayara Chagas Ávila, Plinio Salmazo Vieira, Antonio Bonomi, Gabriela Persinoti, Mario Tyago Murakami, Thomas Michael Makris, Leticia Maria Zanphorlin

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Alkenes have an economic appeal, especially in the biofuels field, since they are precursors for drop-in biofuels production, which have similar chemical and physical properties to the conventional fossil fuels, with no oxygen in their composition. After the discovery of the first P450 CYP152 OleTJE in 2011, reported with its unique property of decarboxylating fatty acids (FA), by using hydrogen peroxide as a cofactor and producing 1-alkenes as the main product, the scientific and technological interest in this family of enzymes vastly increased. In this context, the present work presents a new decarboxylase (OleTRN) with low similarity with OleTJE (32%), its biochemical characterization, and structure elucidation. As main results, OleTRN presented a high yield of expression and purity, optimum reaction conditions at 35 °C and pH from 6.5 to 8.0, and higher specificity for oleic acid. Besides that, structure-guided mutations were performed and according to the functional characterizations, it was observed that some mutations presented different specificity and chemoselectivity by varying the chain-length of FA substrates from 12 to 20 carbons. These results are extremely interesting from a biotechnological perspective as those characteristics could diversify the applications and contribute to designing better cytochrome P450 decarboxylases. Considering that peroxygenases have the potential activity of decarboxylating and hydroxylating fatty acids and that the elucidation of the intriguing mechanistic involved in the decarboxylation preferential from OleTJE is still a challenge, the elucidation of OleTRN structure and the functional characterizations of OleTRN and its mutants contribute to new information about CYP152. Besides that, the work also contributed to the discovery of a new decarboxylase with a different selectivity profile from OleTJE, which allows a wide range of applications.

Keywords: P450, decarboxylases, alkenes, biofuels

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Authors: Khadijat Olabisi Abdulwahab, Mohammad Azad Malik, Paul O'Brien, Grigore Timco, Floriana Tuna

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The synthesis of spinel ferrite nanoparticles with a narrow size distribution is very crucial in their numerous applications including information storage, hyperthermia treatment, drug delivery, contrast agent in magnetic resonance imaging, catalysis, sensors, and environmental remediation. Ferrites have the general formula MFe₂O₄ (M = Fe, Co, Mn, Ni, Zn e.t.c) and possess remarkable electrical and magnetic properties which depend on the cations, method of preparation, size and their site occupancies. To the best of our knowledge, there are no reports on the use of a single source precursor to synthesise quaternary ferrite nanoparticles. Here in, we demonstrated the use of trimetallic iron pivalate cluster [CrCoFeO(O₂CᵗBu)₆(HO₂CᵗBu)₃] as a single source precursor to synthesise monodisperse cobalt chromium ferrite (FeCoCrO₄) nanoparticles by the hot injection thermolysis method. The precursor was thermolysed in oleylamine, oleic acid, with diphenyl ether as solvent at 260 °C. The effect of reaction time on the stoichiometry, phases or morphology of the nanoparticles was studied. The p-XRD patterns of the nanoparticles obtained after one hour was pure phase of cubic iron cobalt chromium ferrite (FeCoCrO₄). TEM showed that a more monodispersed spherical ferrite nanoparticles were obtained after one hour. Magnetic measurements revealed that the ferrite particles are superparamagnetic at room temperature. The nanoparticles were characterised by Powder X-ray Diffraction (p-XRD), Transmission Electron Microscopy (TEM), Energy Dispersive Spectroscopy (EDS) and Super Conducting Quantum Interference Device (SQUID).

Keywords: cobalt chromium ferrite, colloidal, hot injection thermolysis, monodisperse, reaction time, single source precursor, quaternary ferrite nanoparticles

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Authors: Ritu Karwasra, Surender Singh

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Inflammation is an important physiological response of the body’s self-defense system that helps in eliminating and protecting organism from harmful stimuli and in tissue repair. It is a highly regulated protective response which helps in eliminating the initial cause of cell injury, and initiates the process of repair. The present study was designed to evaluate the ameliorative effect of pomegranate rind extract on pain and inflammation. Hydroalcoholic standardized rind extract of pomegranate at doses 50, 100 and 200 mg/kg and indomethacin (3 mg/kg) was tested against eddy’s hot plate induced thermal algesia, carrageenan (acute inflammation) and Complete Freund’s Adjuvant (chronic inflammation) induced models in Wistar rats. Parameters analyzed were inhibition of paw edema, measurement of joint diameter, levels of GSH, TBARS, SOD, TNF-α, radiographic imaging, tissue histology and synovial expression of pro-inflammatory cytokine receptor (TNF-R1). Radiological and light microscopical analysis were carried out to find out the bone damage in CFA-induced chronic inflammatory model. Findings of the present study revealed that pomegranate rind extract at a dose of 200 mg/kg caused a significant (p<0.05) reduction in paw swelling in both the inflammatory models. Nociceptive threshold was also significantly (p<0.05) improved. Immunohistochemical analysis of TNF-R1 in CFA-induced group showed elevated level, whereas reduction in level of TNF-R1 was observed in pomegranate (200 mg/kg). Henceforth, we might say that pomegranate produced a dose-dependent reduction in inflammation and pain along with the reduction in levels of oxidative stress markers and tissue histology, and the effect was found to be comparable to that of indomethacin. Thus, it can be concluded that pomegranate is a potential therapeutic target in the pathogenesis of inflammation and pain, and punicalagin is the major constituents found in rind extract might be responsible for the activity.

Keywords: carrageenan, inflammation, nociceptive-threshold, pomegranate, histopathology

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Authors: Maryam Parsian, Pelin Mutlu, Ufuk Gunduz

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Two-dimensional cell culture affords simplicity and low cost, but it has serious limitations; lacking cell-cell and cell-matrix interactions that are present in tissues. Cancer cells grown in 3D culture systems have distinct phenotypes of adhesion, growth, migration, invasion as well as profiles of gene and protein expression. These interactions cause the 3D-cultured cells to acquire morphological and cellular characteristics relevant to in vivo tumors. Palbociclib is a chemotherapeutic agent for the treatment of ER-positive and HER-negative metastatic breast cancer. Poly-amidoamine (PAMAM) dendrimer is a well-defined, special three-dimensional structure and has a multivalent surface and internal cavities that can play an essential role in drug delivery systems. In this study, palbociclib is loaded onto the magnetic PAMAM dendrimer. Hanging droplet method was used in order to form 3D spheroids. The possible toxic effects of both free drug and drug loaded nanoparticles were evaluated in 2D and 3D MCF-7, MD-MB-231 and SKBR-3 breast cancer cell culture models by performing MTT cell viability and Alamar Blue assays. MTT analysis was performed with six different doses from 1000 µg/ml to 25 µg/ml. Drug unloaded PAMAM dendrimer did not demonstrate significant toxicity on all breast cancer cell lines. The results showed that 3D spheroids are clearly less sensitive than 2D cell cultures to free palbociclib. Also, palbociclib loaded PAMAM dendrimers showed more toxic effect than free palbociclib in all cell lines at 2D and 3D cultures. The results suggest that the traditional cell culture method (2D) is insufficient for mimicking the actual tumor tissue. The response of the cancer cells to anticancer drugs is different in the 2D and 3D culture conditions. This study showed that breast cancer cells are more resistant to free palbociclib in 3D cultures than in 2D cultures. However, nanoparticle loaded drugs can be more cytotoxic when compared to free drug.

Keywords: 2D and 3D cell culture, breast cancer, palbociclibe, PAMAM magnetic nanoparticles

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Authors: Ada Yurman

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Using the case of Israeli Atomic Spy Mordechai Vanunu as an example, this study sought to examine social response to political deviance whereby social response can be mobilized in order to achieve social control. Mordechai Vanunu, a junior technician in the Dimona Atomic Research Center, played a normative role in the militaristic discourse while working in the “holy shrine” of the Israeli defense system for many years. At a certain stage, however, Vanunu decided to detach himself from this collective and launched an assault on this top-secret circle. Israeli society in general and the security establishment in particular found this attack intolerable and unforgivable. They presented Vanunu as a ticking time bomb, delegitimized him and portrayed him as “other”. In addition, Israeli enforcement authorities imposed myriad prohibitions and sanctions on Vanunu even after his release from prison – “as will be done to he who desecrates holiness.” Social response to Vanunu at the time of his capture and trial was studied by conducting a content analysis of six contemporary daily newspapers. The analysis focused on use of language and forms of expression. In contrast with traditional content analysis methodology, this study did not just look at frequency of expressions of ideas and terms in the text and covert content; rather, the text was analyzed as a structural whole, and included examination of style, tone and unusual use of imagery, and more, in order to uncover hidden messages within the text. The social response to this case was extraordinarily intense, not only because in this case of political deviance, involving espionage and treason, Vanunu’s actions comprised a real potential threat to the country, but also because of the threat his behavior posed to the symbolic universe of society. Therefore, the response to this instance of political deviance can be seen as being part of a mechanism of social control aiming to protect world view of society as a whole, as well as to punish the criminal.

Keywords: militarism, political deviance, social construction, social control

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Authors: Tsai Yu-hsin, Chung Yi-Hsin

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The employment of an HSR system, resulting in elevation in the inter-city/-region accessibility, is likely to promote spatial interaction between places in the HSR and extended territory. The inter-city/-region travel via HSR could be, among others, affected by the land use, transportation, and location of the HSR station at both trip origin and destination ends. However, relatively few insights have been shed on these impacts and spatial patterns of the HSR travel. The research purposes, as phase one of a series of HSR related research, of this study are threefold: to analyze the general spatial patterns of HSR trips, such as the spatial distribution of trip origins and destinations; to analyze if specific land use, transportation characteristics, and trip characteristics affect HSR trips in terms of the use of HSR, the distribution of trip origins and destinations, and; to analyze the socio-economic characteristics of HSR travelers. With the Taiwan HSR starting operation in 2007, this study emphasizes on the intermediate-term impact of HSR, which is made possible with the population and housing census and industry and commercial census data and a station area intercept survey conducted in the summer 2014. The analysis will be conducted at the city, inter-city, and inter-region spatial levels, as necessary and required. The analysis tools include descriptive statistics and multivariate analysis with the assistance of SPSS, HLM and ArcGIS. The findings, on the one hand, can provide policy implications for associated land use, transportation plan and the site selection of HSR station. On the other hand, on the travel the findings are expected to provide insights that can help explain how land use and real estate values could be affected by HSR in following phases of this series of research.

Keywords: high speed rail, land use, travel, spatial pattern

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Authors: Lubna Azmi, Ila Shukla, Shyam Sundar Gupta, Padam Kant, Ch. V. Rao

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Gastric ulcer is a major global health threat, and it is the leading cause of stomach cancer death worldwide. Helicobacter pylori bacteriumis the most important etiologic factor for gastric ulcer. This infection is highly pervasive in South Asian developing countries, especially in India, Nepal, Srilanka etc. due to diversification in geographic area. Pathophysiology of gastric mucosal damage associated with non-invasive bacterium has not justified in detail, but it leads to change in histopathology, immunochemistry of the gastric and duodenal reason of host. The mechanism responsible for bacteria tissue tropism and mucosal damage in stomach variance during the disease is not clearly described and understood scientifically in treatment and control of pathogenic organisms. Polyphenols are secondary metabolites of plants and are generally involved in defense against aggression by pathogens. 2-(3,4-dihydroxyphenyl)-3,5,7-trihydroxychromen-4-one and 1-hydroxy-5,7-dimethoxy-2-naphthalene-carboxaldehyde are polyphenolic compound obtained from popular Indian medicinal plants ghavpatta (ArgeriaspeciosaLinn.f) andBael (Aeglemarmelos) have long been used in traditional Ayurvedic Indian medicine for various diseases. They have promising effects on ulcer, as detailed investigation has made in our laboratory. Therefore, the aim of present study is to explore membrane –dependent morphogenesis of H. pylori and associated apoptosis-mediated cell death. Based on this we analyzed immune gene expression in stomach of experimental animals with H. pylori, using quantitative reverse transcription polymerase chain reaction(q RT-PCR). This revealed rapid induction of prostaglandin, interferon I (INF-I), interferon II (INF-II) and INF-I associated genes in the infected animal. Ultrastructural changes associated with H. pylori will be taken for advanced studies. This investigation shows that the biomarkers eradicate H. pylori bacterium caused gastric ulcer which is a major risk factor for gastric cancer.

Keywords: gastric ulcer, Helicobacter pylori, immunochemistry, polyphenols

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Authors: Hyeon Sop Baek

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This paper will briefly investigate Jeong Do-jeon’s political philosophy. Jeong Do-jeon was a Korean Confucian philosopher and politician during the turbulent 14th Century who revolted against the old order, founded Joseon Dynasty, and significantly impacted the development of Korean culture. Jeong’s vision of an ideal state involved a polity that has its roots in the people -that is, an ideal government prioritizes caring for the welfare of the people, respecting and attending to the diverse opinions and concerns of the people, and relies on the genuine, voluntary support of the people. With the neo-Confucian worldview in mind -that every human being has the equal potential to become a moral person- Jeong sought to create a world suitable for everybody to contribute to the decision-making procedure and be able to realize their potential fully. This paper will first examine his works and present a quick overview of his vision of the ideal government. Then, it will examine the Confucian virtues of ren (仁) and yi (義) and how they formulate the basis of his philosophy, and then discuss the central features of his vision of government: popular mandate, equity of wealth, promoting freedom of expression and political participation, and elevating caring disposition as the paramount quality of the political leaders. Furthermore, this paper aims to analyze the element of care inherent within his political philosophy, namely his view on the dynamics of power, nurturing the people, and noncoercive justice. Finally, a discussion on why his philosophy is still relevant in the contemporary context will be provided. Jeong’s view aimed at building a sustainable model of government, by proposing that the people should be the foundation of a state and that they need to be carefully nurtured so they can realize their inborn potential and continue to contribute to the sustenance of the world, is the focal point of Jeong’s philosophy. Just as he sought to rebuild his world following the turmoils of the 14th Century, his philosophy still has a substantial implication on how we should strive to rebuild our society today.

Keywords: Korea, Confucianism, Jeong Do-jeon, Joseon, Korean philosophy, political philosophy

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Authors: Ł. Morawiński, C. Jasiński, M. Jurkiewicz, S. Bou Habib, M. Bondyra

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With the development of optics, electronics, and computers, vision systems are increasingly used in various areas of life, science, and industry. Vision systems have a huge number of applications. They can be used in quality control, object detection, data reading, e.g., QR-code, etc. A large part of them is used for measurement purposes. Some of them make it possible to obtain a 3D reconstruction of the tested objects or measurement areas. 3D reconstruction algorithms are mostly based on creating depth maps from data that can be acquired from active or passive methods. Due to the specific appliance in airfield technology, only passive methods are applicable because of other existing systems working on the site, which can be blinded on most spectral levels. Furthermore, reconstruction is required to work long distances ranging from hundreds of meters to tens of kilometers with low loss of accuracy even with harsh conditions such as fog, rain, or snow. In response to those requirements, HRESS (Heliport REmote Safeguard System) was developed; which main part is a rotational head with a two-camera stereovision rig gathering images around the head in 360 degrees along with stereovision 3D reconstruction and point cloud combination. The sub-pixel analysis introduced in the HRESS system makes it possible to obtain an increased distance measurement resolution and accuracy of about 3% for distances over one kilometer. Ultimately, this leads to more accurate and reliable measurement data in the form of a point cloud. Moreover, the program algorithm introduces operations enabling the filtering of erroneously collected data in the point cloud. All activities from the programming, mechanical and optical side are aimed at obtaining the most accurate 3D reconstruction of the environment in the measurement area.

Keywords: airfield monitoring, artificial intelligence, stereovision, 3D reconstruction

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Authors: Eric Lai, Sarah Lorger, David Eisinger, Richard Waugh

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Introduction: Percutaneous embolization of varicoceles has shown similar outcomes to surgery. However, there are advantages of radiological intervention as patients are not exposed to general anaesthesia, experience a quicker recovery and face a lower risk of major complications. Radiological interventions are also preferable after a failed surgical approach. We evaluate clinical outcomes of percutaneous embolization at a tertiary hospital in Sydney, Australia. Methods: Retrospective case series without a control group from a single site (Royal Prince Alfred Hospital, Sydney, Australia). A data search was performed on the interventional radiology database with the word “varicocele” between February 2017 and March 2022. 62 patients were identified. Each patient file was reviewed and included in the study if they met the inclusion criteria. Results: A total of 56 patients were included. 6 patients were excluded as they did not receive intervention after the initial diagnostic venography. Technical success was 100%. Complications were seen in 3 patients (5.3%). The complications included post-procedural pain and fever, venous perforation with no clinical adverse outcome, and a mild allergic reaction to contrast. Recurrence occurred in 3 patients (5.6%), all of whom received a successful second procedure. DISCUSSION: This study demonstrates comparable rates of technical success, complication rate and recurrence to other studies in the literature. When compared to surgical outcomes, the results were also similar. The main limitation is multiple patients lack long-term follow-up beyond 1 year, resulting in potential underestimation of the recurrence rate. Conclusion: Percutaneous embolization of varicocele is a safe alternative to surgical intervention.

Keywords: varicocele, interventional radiology, urology, radiology

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Authors: Shanakr Bhattarai, V. S. Tiwari, Barak Akabayov

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The plummeting number of infections and death is due to the development of drug-resistant bacteria. In addition, the number of approved antibiotic drugs by the Food and Drug Administration (FDA) is insufficient. Therefore, developing new drugs and finding novel targets for central metabolic pathways in bacteria is urgently needed. One of the promising targets is DNA replication machinery which consists of many essential proteins and enzymes. DnaG primase is an essential enzyme and a central part of the DNA replication machinery. DnaG primase synthesizes short RNA primers that initiate the Okazaki fragments by the lagging strand DNA polymerase. Therefore, it is reasonable to assume that inhibition of primase activity will stall DNA replication and prevent bacterial proliferation. We did the expression and purification of eight different bacterial DnaGs (Mycobacterium tuberculosis(Mtb), Bacillus anthracis (Ba), Mycobacterium smegmatis (Msmeg), Francisella tularencis (Ft), Vibrio cholerae (Vc) and Yersinia pestis (Yp), Staphylococcus aureus(Saureus), Escherichia coli(Ecoli)) followed by the radioactive activity assay. After obtaining the pure and active protein DnaG, we synthesized the inhibitors for them. The inhibitors were divided into five different groups, each containing five molecules, and the cocktail inhibition assay was performed against each DnaGs. The groups of molecules inhibiting the DnaGs were further tested with individual molecules belonging to inhibiting groups. Each molecule showing inhibition was titrated against the corresponding DnaGs to find IC50. We got a molecule(VS167) that acted as broad inhibitors, inhibiting all eight DnaGs. Molecules VS180 and VS186 inhibited seven DnaGs (except Saureus). Similarly, two molecules(VS 173, VS176) inhibited five DnaGs (Mtb, Ba, Ft, Yp, Ecoli). VS261 inhibited four DnaGs (Mtb, Ba, Ft, Vc). MS50 inhibited Ba and Vc DnaGs. And some of the inhibitors inhibited only one DnaGs. Thus we found the broad and specific inhibitors for different bacterial DnaGs, and their Structure-activity analysis(SAR) was done. Further, We tried to explain the similarities among the enzyme DnaGs from different bacteria based on their inhibition pattern.

Keywords: DNA replication, DnaG, okazaki fragments, antibiotic drugs

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Authors: Gebreslassie Gebru, Gurja Belay, Minister Birhanie, Mulalem Zenebe, Tadelle Dessie, Adriana Vallejo-Trujillo, Olivier Hanotte

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Livestock must adapt to changing environmental conditions, which can result in either phenotypic plasticity or irreversible phenotypic change. In this study, we combine Ecological Niche Modelling (ENM) and Phenotypic Distribution Modelling (PDM) to provide a comprehensive framework for understanding the ecological and phenotypic characteristics of indigenous chicken (Gallus gallus domesticus) ecotypes. This approach helped us to classify these ecotypes, differentiate their phenotypic traits, and identify associations between environmental variables and adaptive traits. We measured 297 adult indigenous chickens from various agro-ecologies, including 208 females and 89 males. A subset of the 22 measured traits was selected using stepwise selection, resulting in seven traits for each sex. Using ENM, we identified four agro-ecologies potentially harbouring distinct phenotypes of indigenous Tigray chickens. However, PDM classified these chickens into three phenotypical ecotypes. Chickens grouped in ecotype-1 and ecotype-3 exhibited superior adaptive traits compared to those in ecotype-2, with significant variance observed. This high variance suggests a broader range of trait expression within these ecotypes, indicating greater adaptation capacity and potentially more diverse genetic characteristics. Several environmental variables, such as soil clay content, forest cover, and mean temperature of the wettest quarter, were strongly associated with most phenotypic traits. This suggests that these environmental factors play a role in shaping the observed phenotypic variations. By integrating ENM and PDM, this study enhances our understanding of indigenous chickens' ecological and phenotypic diversity. It also provides valuable insights into their conservation and management in response to environmental changes.

Keywords: adaptive traits, agro-ecology, appendage, climate, environment, imagej, morphology, phenotypic variation

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Authors: K. Vrinda

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Coastal ecosystems across the world are facing a lot of challenges due to natural phenomena as well as from uncontrolled human interventions. Here, Alappad, a coastal island situated in Kerala, India is undergoing significant damage and is gradually losing its environmental and social sustainability. The area is blessed with very rare and precious black mineral sand deposits. Sand mining for these minerals started in 1911 and is still continuing. But, unfortunately all the problems that Alappad faces now, have its root on mining of this mineral sand. The land area is continuously diminishing due to sea erosion. The mining has also caused displacement of people and environmental degradation. Marine life also is getting affected by mining on beach and pollution. The inhabitants are fishermen who are largely dependent on the eco-system for a living. So loss of environmental sustainability subsequently affects social sustainability too. Now the damage has reached a point beyond which our actions may not be able to make any impact. This was one of the most affected areas of the 2004 tsunami and the environmental degradation has further increased the vulnerability. So this study focuses on understanding the concerns related to the resource utilization, environment and the indigenous community staying there, and on formulating suitable strategies to restore the sustainability of the area. An extensive study was conducted on site, to find out the physical, social, and economical characteristics of the area. A focus group discussion with the inhabitants shed light on different issues they face in their day-to-day life. The analysis of all these data, led to the formation of a new development vision for the area which focuses on environmental restoration and socio-economic development while allowing controlled exploitation of resources. A participatory approach is formulated which enables these three aspects through community based programs.

Keywords: Community development, Disaster resilience, Ecological restoration, Environmental sustainability, Social-environmental planning, Social Sustainability

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Authors: Akanimo Emene, Robert Edyvean

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In developing countries, a low cost method of wastewater treatment is highly recommended. Adsorption is an efficient and economically viable treatment process for wastewater. The utilisation of this process is based on the understanding of the relationship between the growth environment and the metal capacity of the biomaterial. Luffa cylindrica (LC), a plant material, was used as an adsorbent in adsorption design system of heavy metals. The chemically modified LC was used to adsorb heavy metals ions, lead and cadmium, from aqueous environmental solution at varying experimental conditions. Experimental factors, adsorption time, initial metal ion concentration, ionic strength and pH of solution were studied. The chemical nature and surface area of the tissues adsorbing heavy metals in LC biosorption systems were characterised by using electron microscopy and infra-red spectroscopy. It showed an increase in the surface area and improved adhesion capacity after chemical treatment. Metal speciation of the metal ions showed the binary interaction between the ions and the LC surface as the pH increases. Maximum adsorption was shown between pH 5 and pH 6. The ionic strength of the metal ion solution has an effect on the adsorption capacity based on the surface charge and the availability of the adsorption sites on the LC. The nature of the metal-surface complexes formed as a result of the experimental data were analysed with kinetic and isotherm models. The pseudo second order kinetic model and the two-site Langmuir isotherm model showed the best fit. Through the understanding of this process, there will be an opportunity to provide an alternative method for water purification. This will be provide an option, for when expensive water treatment technologies are not viable in developing countries.

Keywords: adsorption, luffa cylindrica, metal-surface complexes, pH

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Authors: Nguyen Chi Quang, Nguyen Duong Tri Nguyen

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This article is the first step to research and outline the structure of the geotechnical database in the geological survey of a power project; in the context of this report creating the database that has been carried out for the Bac Ai pumped storage hydropower project. For the purpose of providing a method of organizing and storing geological and topographic survey data and experimental results in a spatial database, the RockWorks software is used to bring optimal efficiency in the process of exploiting, using, and analyzing data in service of the design work in the power engineering consulting. Three-dimensional (3D) geotechnical models are created from the survey data: such as stratigraphy, lithology, porosity, etc. The results of the 3D geotechnical model in the case of Bac Ai pumped storage hydropower project include six closely stacked stratigraphic formations by Horizons method, whereas modeling of engineering geological parameters is performed by geostatistical methods. The accuracy and reliability assessments are tested through error statistics, empirical evaluation, and expert methods. The three-dimensional model analysis allows better visualization of volumetric calculations, excavation and backfilling of the lake area, tunneling of power pipelines, and calculation of on-site construction material reserves. In general, the application of engineering geological modeling makes the design work more intuitive and comprehensive, helping construction designers better identify and offer the most optimal design solutions for the project. The database always ensures the update and synchronization, as well as enables 3D modeling of geological and topographic data to integrate with the designed data according to the building information modeling. This is also the base platform for BIM & GIS integration.

Keywords: database, engineering geology, 3D Model, RockWorks, Bac Ai pumped storage hydropower project

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Authors: Arda Bagus M, Yehezkiel Festian P, Budianto Santoso

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The Tourism Area of Southern Malang is administratively located in the Regency of Malang, East Java Province, Indonesia and geographically is in a position between 112o17' - 112o57' E dan 7o44' - 8o26' S. Southern Malang consists of several sub-districts that directly borders with the Indian Ocean, such as Donomulyo, Bantur, Gedangan, Sumbermanjing, Tirto Yudo, and Ampel Gading. This area has a high geotourism potential because of the existence of geodiversity such as beaches, waterfalls, caves, and karst area. However, to the best of the authors’ knowledge, there is still no systematic data that informs the geotourism potentials to the public. The aim of this research is to complete the lack of data and then arrange it systematically so it can be used for both tourism and research purposes. Research methods such as field observation, literature study, and depth interview to local people have been implemented. Aspects reviewed by visiting the field are accommodation, transportation, and the feasibility of a place to be geotourism object. The primary data was taken in Sumbermanjing, Gedangan, Bantur, and Donomulyo sub-district. A literature study is needed to determine the regional geology of Southern Malang and as a comparison to new data obtained in the field. The results of the literature study show that southern Malang consists of three formations: Wonosari Formation, Mandalaka Formation, and River-swamps Sediment Formation with the age range of Oligocene to Quaternary. Depth interviews have been conducted by involving local people with the aim of knowing cultural-history in the research area. From this research, the geotourism object distribution map has been made. The map also includes Geotrek and basic geological information of each object. The results of this research can support the development of geotourism in Southern Malang.

Keywords: geodiversity, geology, geotourism, geotrek, southern Malang

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Authors: Hasan Frookh Jamal

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This is a case of a 36-year-old Bahraini gentleman diagnosed to have Cushing's Syndrome with a large anterior mediastinal mass. He was sent abroad to the Speciality hospital in Jordan, where he underwent diagnostic video-assisted thoracoscopy, partial thymectomy and pericardial fat excision. Histopathology of the mass was reported to be an Atypical carcinoid tumor with a low Ki67 proliferation index of 5%, the mitotic activity of 4 MF/10HPF and pathological stage classification(pTNM): pT1aN1. MRI of the pituitary gland showed an ill-defined non-enhancing focus of about 3mm on the Rt side of the pituitary on coronal images, with a similar but smaller one on the left side, which could be due to enhancing pattern rather than a real lesion as reported. The patient underwent Ga68 Dotate PET/CT scan post-operatively, which showed multiple somatostatin receptor-positive lesions seen within the tail, body and head of the pancreas and positive somatostatin receptor lymph nodes located between the pancreatic head and IVC. There was no uptake detected at the anterior mediastinum nor at the site of thymic mass resection. There was no evidence of any positive somatostatin uptake at the soft tissue or lymph nodes. The patient underwent IPSS, which proved that the source is, in fact, an ectopic source of ACTH secretion. Unfortunately, the patient's serum cortisol remained elevated after surgery and failed to be suppressed by 1 mg ODST and by 2 days LLDST with a high ACTH value. The patient was started on Osilodrostat for treatment of hypercortisolism for the time being and his future treatment plan with Lutetium-177 Dotate therapy vs. bilateral adrenalectomy is to be considered in an MDT meeting.

Keywords: cushing syndrome, neuroendocrine tumur, carcinoid tumor, Thymoma

Procedia PDF Downloads 83

Authors: Ilyasu G., Ogoina D., Otu AA, Muhammed FD, Ebenso B., Otokpa D., Rotifa S., Tuduo-Wisdom O., Habib AG

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Background: The 2014 Ebola Virus Disease (EVD) outbreak was characterized by fear, misconceptions and irrational behaviors. We conducted a knowledge attitude and practice survey of EVD in Nigeria to inform the institution of effective control measures. Methods: Between July 30th and September 30th 2014, a cross-sectional study on knowledge, attitude and practice (KAP) of Ebola Virus Disease (EVD) was undertaken among adults of the general population and healthcare workers (HCW) in three states of Nigeria, including Kano, Cross River and Bayelsa states. Demographic information and data on KAP were obtained using a self-administered standardized questionnaire. The percentage KAP scores were categorized as good and poor. Independent predictors of good knowledge of EVD were ascertained using a binary logistic regression model. Results: Out of 1035 study participants with a median age of 32 years, 648 (62.6%) were males, 846 (81.7%) had tertiary education and 441 (42.6%) were HCW. There were 218, 239 and 578 respondents from Bayelsa, Cross Rivers, and Kano states, respectively. The overall median percentage KAP scores and interquartile ranges (IQR) were 79.46% (15.07%), 95.0% (33.33%), and 49.95% (37.50%), respectively. Out of the 1035 respondents, 470 (45.4%), 544(52.56%), and 252 (24.35%) had good KAP of EVD defined using 80%, 90%, and 70% score cut-offs, respectively. Independent predictors of good knowledge of EVD were a HCW (Odds Ratio-OR-2.89, 95% Confidence interval-CI of 1.41-5.90), reporting ‘moderate to high fear of EVD’ (OR-2.15, 95% CI-1.47-3.13) and ‘willingness to modify habit’ (OR-1.68, 95% CI-1.23-2.30). Conclusion: Our results reveal suboptimal EVD-related knowledge, attitude and practice among adults in Nigeria. To effectively control future outbreaks of EVD in Nigeria, there is a need to institute public sensitization programs that improve understanding of EVD and address EVD-related myths and misconceptions, especially among the general population.

Keywords: Ebola, health care worker, knowledge, attitude

Procedia PDF Downloads 286

Authors: Ruqaiya Khalil, Saman Usmani, Zaheer Ul-Haq

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The accurate characterization of ligand binding affinity is indispensable for designing molecules with optimized binding affinity. Computational tools help in many directions to predict quantitative correlations between protein-ligand structure and their binding affinities. Molecular dynamics (MD) simulation is a modern state-of-the-art technique to evaluate the underlying basis of ligand-protein interactions by characterizing dynamic and energetic properties during the event. Autoimmune diseases arise from an abnormal immune response of the body against own tissues. The current regimen for the described condition is limited to immune-modulators having compromised pharmacodynamics and pharmacokinetics profiles. One of the key player mediating immunity and tolerance, thus invoking autoimmunity is Interleukin-2; a cytokine influencing the growth of T cells. Molecular dynamics simulation techniques are applied to seek insight into the inhibitory mechanisms of newly synthesized compounds that manifested immunosuppressant potentials during in silico pipeline. In addition to estimation of free energies associated with ligand binding, MD simulation yielded us a great deal of information about ligand-macromolecule interactions to evaluate the pattern of interactions and the molecular basis of inhibition. The present study is a continuum of our efforts to identify interleukin-2 inhibitors of both natural and synthetic origin. Herein, we report molecular dynamics simulation studies of Interluekin-2 complexed with different antagonists previously reported by our group. The study of protein-ligand dynamics enabled us to gain a better understanding of the contribution of different active site residues in ligand binding. The results of the study will be used as the guide to rationalize the fragment based synthesis of drug-like interleukin-2 inhibitors as immune-modulators.

Keywords: immuno-modulators, MD simulation, protein-ligand interaction, structure-based drug design

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Authors: Khadijat O. Abdulwahab, Mohammad A. Malik, Paul O’Brien, Grigore A. Timco, Floriana Tuna

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The synthesis of spinel ferrite nanoparticles with a narrow size distribution is very crucial in their numerous applications including information storage, hyperthermia treatment, drug delivery, contrast agent in magnetic resonance imaging, catalysis, sensors, and environmental remediation. Ferrites have the general formula MFe2O4 (M = Fe, Co, Mn, Ni, Zn etc.) and possess remarkable electrical and magnetic properties which depend on the cations, method of preparation, size and their site occupancies. To the best of our knowledge, there are no reports on the use of a single source precursor to synthesise quaternary ferrite nanoparticles. Herein, we demonstrated the use of trimetallic iron pivalate cluster [CrCoFeO(O2CtBu)6(HO2CtBu)3] as a single source precursor to synthesise monodisperse cobalt chromium ferrite (FeCoCrO4) nanoparticles by the hot injection thermolysis method. The precursor was thermolysed in oleylamine, oleic acid, with diphenyl ether as solvent at its boiling point (260°C). The effect of concentration on the stoichiometry, phases or morphology of the nanoparticles was studied. The p-XRD patterns of the nanoparticles obtained at both concentrations were matched with cubic iron cobalt chromium ferrite (FeCoCrO4). TEM showed that a more monodispersed spherical ferrite nanoparticles of average diameter 4.0 ± 0.4 nm were obtained at higher precursor concentration. Magnetic measurements revealed that all the ferrite particles are superparamagnetic at room temperature. The nanoparticles were characterised by Powder X-ray Diffraction (p-XRD), Transmission Electron Microscopy (TEM), Inductively Coupled Plasma (ICP), Electron Probe Microanalysis (EPMA), Energy Dispersive Spectroscopy (EDS) and Super Conducting Quantum Interference Device (SQUID).

Keywords: quaternary ferrite nanoparticles, single source precursor, monodisperse, cobalt chromium ferrite, colloidal, hot injection thermolysis

Procedia PDF Downloads 276

Authors: Nowbuth Manta Devi, Rasmally Mohammed Hussein

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Flood is one of the most devastating climate impacts that many countries are facing. Many different causes have been associated with the intensity of floods being recorded over time. Unplanned development, low carrying capacity of drains, clogged drains, construction in flood plains or increasing intensity of rainfall events. While a combination of these causes can certainly aggravate the flood conditions, in many cases, increasing drainage capacity has not reduced flood risk to the level that was expected. The present study analyzed the extent to which land use is contributing to aggravating impacts of flooding in a city. Satellite images have been analyzed over a period of 20 years at intervals of 5 years. Both unsupervised and supervised classification methods have been used with the image processing module of ArcGIS. The unsupervised classification was first compared to the basemap available in ArcGIS to get a first overview of the results. These results also aided in guiding data collection on-site for the supervised classification. The island of Mauritius is small, and there are large variations in land use over small areas, both within the built areas and in agricultural zones involving food crops. Larger plots of agricultural land under sugar cane plantations are relatively more easily identified. However, the growth stage and health of plants vary and this had to be verified during ground truthing. The results show that although there have been changes in land use as expected over a span of 20 years, this was not significant enough to cause a major increase in flood risk levels. A digital elevation model was analyzed for further understanding. It could not be noted that overtime, development tampered with natural flow paths in addition to increasing the impermeable areas. This situation results in backwater flows, hence increasing flood risks.

Keywords: climate change, flood, natural flow paths, small islands

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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 247