Search results for: nitrification inhibitor and nitrogen use efficiency
Commenced in January 2007
Frequency: Monthly
Edition: International
Paper Count: 7600

Search results for: nitrification inhibitor and nitrogen use efficiency

6760 Promotion of Renewable Marines Energies in Morocco: Perspectives and Strategies

Authors: Nachtane Mourad, Tarfaoui Mostapha, Saifaoui Dennoun, El Moumen Ahmed

Abstract:

The current energy policy recommends the subject of energy efficiency and to phase out fossil energy as a master question for the prospective years. The kingdom requires restructuring its power equipment by improving the percentage of renewable energy supply and optimizing power systems and storage. Developing energy efficiency, therefore, obliges as a consubstantial objection to reducing energy consumption. The objective of this work is to show the energy transition in Morocco towards renewable energies, in particular, to show the great potential of renewable marine energies in Morocco, This goes back to the advantages of cost and non-pollution in addition to that of the independence of fossil energies. Bearing in mind the necessity of the balance of the Moroccan energy mix, hydraulic and thermal power plants have also been installed which will be added to the power stations already established as a prospect for a balanced network that is flexible to fluctuate demand.

Keywords: renewable marine energy, energy transition, efficiency energy, renewable energy

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6759 Proposals for the Thermal Regulation of Buildings in Algeria: A New Energy Label for Social Housing

Authors: Marco Morini, Nicolandrea Calabrese, Dario Chello

Abstract:

Despite the international commitment of Algeria towards the development of energy efficiency and renewable energy in the country, the internal energy demand has been continuously growing during the last decade due to the substantial increase of population and of living conditions, which in turn has led to an unprecedented expansion of the residential building sector. The thermal building regulation is the technical document that establishes the calculation framework for the thermal performance of buildings in Algeria, setting up minimum obligatory targets for the thermal performance of new buildings. An update of this regulation is due in the coming years, and this paper discusses some proposals in this regard, with the aim to improve the energy efficiency of the building sector, particularly with regard to social housing. In particular, it proposes a methodology for drafting an energy performance label of new Algerian residential buildings, moving from the results of the thermal compliance verification and sizing of technical systems as defined in the RTB. Such an energy performance label – whose calculation method is briefly described in the paper – aims to raise citizens' awareness of the benefits of energy efficiency. It can represent the first step in a process of integrating technical installations into the calculation of the energy performance of buildings in Algeria.

Keywords: building, energy certification, energy efficiency, social housing, international cooperation, Mediterranean region

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6758 A Key Parameter in Ocean Thermal Energy Conversion Plant Design and Operation

Authors: Yongjian Gu

Abstract:

Ocean thermal energy is one of the ocean energy sources. It is a renewable, sustainable, and green energy source. Ocean thermal energy conversion (OTEC) applies the ocean temperature gradient between the warmer surface seawater and the cooler deep seawater to run a heat engine and produce a useful power output. Unfortunately, the ocean temperature gradient is not big. Even in the tropical and equatorial regions, the surface water temperature can only reach up to 28oC and the deep water temperature can be as low as 4oC. The thermal efficiency of the OTEC plants, therefore, is low. In order to improve the plant thermal efficiency by using the limited ocean temperature gradient, some OTEC plants use the method of adding more equipment for better heat recovery, such as heat exchangers, pumps, etc. Obviously, the method will increase the plant's complexity and cost. The more important impact of the method is the additional equipment needs to consume power too, which may have an adverse effect on the plant net power output, in turn, the plant thermal efficiency. In the paper, the author first describes varied OTEC plants and the practice of using the method of adding more equipment for improving the plant's thermal efficiency. Then the author proposes a parameter, plant back works ratio ϕ, for measuring if the added equipment is appropriate for the plant thermal efficiency improvement. Finally, in the paper, the author presents examples to illustrate the application of the back work ratio ϕ as a key parameter in the OTEC plant design and operation.

Keywords: ocean thermal energy, ocean thermal energy conversion (OTEC), OTEC plant, plant back work ratio ϕ

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6757 An Evaluation of the Impact of E-Banking on Operational Efficiency of Banks in Nigeria

Authors: Ibrahim Rabiu Darazo

Abstract:

The research has been conducted on the impact of E-banking on the operational efficiency of Banks in Nigeria, A case of some selected banks (Diamond Bank Plc, GTBankPlc, and Fidelity Bank Plc) in Nigeria. The research is a quantitative research which uses both primary and secondary sources of data collection. Questionnaire were used to obtained accurate data, where 150 Questionnaire were distributed among staff and customers of the three Banks , and the data collected where analysed using chi-square, whereas the secondary data where obtained from relevant text books, journals and relevant web sites. It is clear from the findings that, the use of e-banking by the banks has improved the efficiency of these banks, in terms of providing efficient services to customers electronically, using Internet Banking, Telephone Banking ATMs, reducing time taking to serve customers, e-banking allow new customers to open an account online, customers have access to their account at all the time 24/7.E-banking provide access to customers information from the data base and cost of check and postage were eliminated using e-banking. The recommendation at the end of the research include; the Banks should try to update their electronic gadgets, e-fraud(internal & external) should also be controlled, Banks shall employ qualified man power, Biometric ATMs shall be introduce to reduce fraud using ATM Cards, as it is use in other countries like USA.

Keywords: banks, electronic banking, operational efficiency of banks, biometric ATMs

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6756 Readiness Assessment to Implement Net-Zero Energy Building Program of Government Buildings in the Philippines

Authors: Patrick T. Aquino, Jimwel B. Balunday, Cephas Olivier V. Cabatit, Mary Grace Q. Razonable

Abstract:

In 2023, the Philippine Department of Energy (PDOE) published the National Energy Efficiency and Conservation Plan (NEECP) and Roadmap 2023-2050 to be the basis of a comprehensive program for the efficient supply and economical use of energy. The building sector, as one of the most energy-intensive sectors, shall conform to the energy-conserving design to reduce the use of energy. The concept of Net-Zero Energy Building (NZEB), and its definitions promote to improve energy efficiency of the buildings. The PDOE partnered with Meralco Power Academy to survey and conduct focus group discussions to establish the readiness into NZE-aspiring buildings of government entities. This paper outlines important NZEB principles, best practices from other countries, issues and gaps relating to energy management program, and the recommendations on the development of a framework for NZEB under government building in the Philippines. Results revealed the limitation on specific data to establish a baseline building energy efficiency performance index and significant energy uses; the need to update the Guidelines for Energy Conservation Design of Buildings, including NZEB definition and requirements; appropriate enabling infrastructures and programs to transition government buildings into NZE-aspiring buildings to Nearly Zero Energy Buildings by 2050.

Keywords: NZEB, energy efficiency, buildings, Philippines

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6755 Biodegrading Potentials of Plant Growth - Promoting Bacteria on Insecticides Used in Agricultural Soil

Authors: Chioma Nwakanma, Onyeka Okoh Irene, Emmanuel Eze

Abstract:

Pesticide residues left in agricultural soils after cropping are always accumulative, difficult to degrade and harmful to animals, plants, soil and human health in general. The biodegrading potential of pesticides- resistant PGPB on soil pollution was investigated using in situ remediation technique following recommended standards. In addition, screening for insecticide utilization, maximum insecticide concentration tolerance, insecticide biodegradation and insecticide residues analyses via gas chromatographic/electron column detector were determined. The location of bacterial degradation genes was also determined. Three plant growth-promoting rhizophere (PGPR) were isolated and identified according to 16S rRNA as Paraburkholderia tropica, Burkolderia glumae and Achromobacter insolitus. From the results, all the three isolates showed phosphate solubilizing traits and were able to grow on nitrogen free medium. The isolates were able to utilize the insecticide as sole carbon source and increase in biomass. They were statistically significantly tolerant to all the insecticide concentrations screened. The gas chromatographic profiles of the insecticide residues showed a reduction in the peak areas of the insecticides, indicating degradation. The bacterial consortium had the lowest peak areas, showing the highest degradation efficiency. The genes responsible for degradation were found to be in the plasmids of the isolates. Therefore, the use of PGPR is recommended for bioremediation of agricultural soil insecticide polluted areas and can also enhance soil fertility.

Keywords: biodegradation, rhizosphere, insecticides utilization, agricultural soil

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6754 Photocatalysis with Fe/Ti-Pillared Clays for the Oxofunctionalization of Alkylaromatics by O2

Authors: Houria Rezala, Jose Luis Valverde, Amaya Romero, Alessandra Molinari, Andrea Maldotti

Abstract:

A pillared montmorillonite containing iron doped titania (Fe/Ti-PILC) has been prepared from a natural clay. This material has been characterized by X-ray diffraction, nitrogen adsorption, temperature programmed desorption of ammonia, inductively coupled plasma atomic emission spectroscopy, atomic absorption, and diffuse reflectance UV-VIS spectroscopy. The layer structure of Fe/Ti-PILC resulted to be ordered with an insertion of pillars, which caused a slight increase in the basal spacing of the clay. Its specific surface area was about three times larger than that of the parent Na-montmorillonite due principally to the creation of a remarkable microporous network. The doped material was a robust photocatalyst able to oxidize liquid alkyl aromatics to the corresponding carbonylic derivatives, using O2 as the oxidizing species, at mild pressure and temperature conditions. Accumulation of valuable carbonylic derivatives was possible since their over-oxidation to carbon dioxide was negligible. Fe/Ti-PILC was able to discriminate between toluene and cyclohexane in favor of the aromatic compound with an efficiency that is about three times higher than that of titanium pillared clays (Ti-PILC). It is likely that the addition of iron favored the formation of new acid sites able to interact with the aromatic substrate. Iron doping caused a significant TiO2 visible light-induced activity (wavelength > 400 nm) with only minor negative effects on its performance under UV-light irradiation (wavelength > 290 nm).

Keywords: alkyl aromatics oxidation, heterogeneous photocatalysis, iron doping, pillared clays

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6753 Study of Suezmax Shuttle Tanker Energy Efficiency for Operations at the Brazilian Pre-Salt Region

Authors: Rodrigo A. Schiller, Rubens C. Da Silva, Kazuo Nishimoto, Claudio M. P. Sampaio

Abstract:

The need to reduce fossil fuels consumption due to the current scenario of trying to restrain global warming effects and reduce air pollution is dictating a series of transformations in shipping. This study introduces, at first, the changes of the regulatory framework concerning gas emissions control and fuel consumption efficiency on merchant ships. Secondly, the main operational procedures with high potential reduction of fuel consumption are discussed, with focus on existing vessels, using ship speed reduction procedure. This procedure shows the positive impacts on both operating costs reduction and also on energy efficiency increase if correctly applied. Finally, a numerical analysis of the fuel consumption variation with the speed was carried out for a Suezmax class oil tanker, which has been adapted to oil offloading operations for FPSOs in Brazilian offshore oil production systems. In this analysis, the discussions about the variations of vessel energy efficiency from small speed rate reductions and the possible applications of this improvement, taking into account the typical operating profile of the vessel in such a way to have significant economic impacts on the operation. This analysis also evaluated the application of two different numerical methods: one based only on regression equations produced by existing data, semi-empirical method, and another using a CFD simulations for estimating the hull shape parameters that are most relevant for determining fuel consumption, analyzing inaccuracies and impact on the final results.

Keywords: energy efficiency, offloading operations, speed reduction, Suezmax oil tanker

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6752 Attaining Financial Efficiency through Funds Utilization

Authors: Muhammad Shujaat Saleem, Imamuddin

Abstract:

In reply to the argument made by the non-believers of Makkah “Sale is similar to riba”, Almighty Allah ordered “Sale is permissible while riba is impermissible”. The main intent of the study was to clarify the fallacy prevailing among the Muslims that in practical terms the product of Murabaha which is being offered by the Islamic banks is similar to that of conventional interest based business loan. However, specific objective was to ascertain the degree of financial efficiency on the basis of fund/loan utilization for intended purpose of Murabaha financing vis-à-vis conventional interest based business loan. The study employed survey strategy to collect primary data through structured close ended questionnaires from the sample of 98 Murabaha officers and 178 loan officers out of the whole population of 5 Islamic and 10 conventional banks respectively. Quantitative and qualitative techniques were used to analyze the data and the same is tabulated by use of frequency tables. The study found that the financial efficiency of Murabaha financing is more than that of conventional interest based business loan by 28% as Murabaha funds of Islamic banks are utilized for its intended purpose to the extent of 97% on average, compared to 69% of business loan offered by conventional banks.

Keywords: financial efficiency, murabaha funds, loan amount, intended purpose

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6751 Improvement of Production of γ-Aminobutyric Acid by Lactobacillus plantarum Isolated from Indigenous Fermented Durian (Tempoyak)

Authors: Yetti Marlida, Harnentis, Yuliaty Shafan Nur

Abstract:

Background: Tempoyak is a dish derived from fermented durian fruit. Tempoyak is a food consumed as a side dish when eating rice. Besides being eaten with rice, tempoyak can also be eaten directly. But this is rarely done because many cannot stand the sour taste and aroma of the tempoyak itself. In addition, tempoyak can also be used as a seasoning. The taste of tempoyak is acidic, this occurs because of the fermentation process in durian fruit meat which is the raw material. Tempoyak is already very well known in Indonesia, especially in Padang, Bengkulu, Palembang, Lampung, and Kalimantan. Besides that, this food is also famous in Malaysia. The purpose of this research is to improvement production of γ-aminobutyric acid (GABA) by Lactobacillus plantarum isolated from indigenous fermented durian (tempoyak). Selected Lactic Acid Bacteria (LAB) previously isolated from indigenous fermented durian (tempoyak) that have ability to produce γ-aminobutyric acid (GABA). The study was started with identification of selected LAB by 16 S RNA, followed optimation of GABA production by culture condition using different initial pH, temperature, glutamate concentration, incubation time, carbon and nitrogen sources. Results: The result from indentification used polymerase chain reaction of 16S rRNA gene sequences and phylogenetic analysis was Lactobacillus plantarum (coded as Y3) with a sequenced length of 1400bp. The improvement of Gaba production was found highest at pH: 6.0; temperature: 30 °C; glutamate concentration: 0.4%; incubation time: 60 h; glucose and yeast extract as carbon and nitrogen sources. Conclusions: GABA can be produced with the optimum condition fermentation were 66.06 mM.

Keywords: lactic acid bacteria, γ-amino butyric acid, indigenous fermented durian, PCR

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6750 Technical Efficiency of Small-Scale Honey Producer in Ethiopia: A Stochastic Frontier Analysis

Authors: Kaleb Shiferaw, Berhanu Geberemedhin

Abstract:

Ethiopian farmers have a long tradition of beekeeping and the country has huge potential for honey production. However traditional mode of production still dominates the sub sector which negatively affect the total production and productivity. A number of studies have been conducted to better understand the working honey production, however, none of them systematically investigate the extent of technical efficiency of the sub-sector. This paper uses Stochastic Frontier production model to quantifying the extent of technical efficiency and identify exogenous determinant of inefficiency. The result showed that consistent with other studies traditional practice dominate small scale honey production in Ethiopia. The finding also revealed that use of purchased inputs such as bee forage and other supplement is very limited among honey producers indicating that natural bee forage is the primary source of bee forage. The immediate consequence of all these is low production and productivity. The number of hives the household owns, whether the household used improved apiculture technologies, availability of natural forest which is the primary sources of nectar for bees and amount of land owned by the households were found to have a significant influence on the amount of honey produced by beekeeper. Our result further showed that the mean technical efficiency of honey producers is 0.79 implying that, on average honey producer produce 80 percent of the maximum output. The implication is that 20 percent of the potential output is lost due to technical inefficiency. Number of hives owned by a honey produces, distance to district town-a proxy to market access, household wealth, and whether the household head has a leadership role in the PA affect the technical efficiency of honey producers. The finding suggest that policies that aim to expand the use of improved hives is expected to increase the honey production at household level. The result also suggest that investment on rural infrastructure would be instrumental in improving technical efficiency of honey producer.

Keywords: small-scale honey producer, Ethiopia, technical efficiency in apiculture, stochastic frontier analysis

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6749 Effect of Three Drying Methods on Antioxidant Efficiency and Vitamin C Content of Moringa oleifera Leaf Extract

Authors: Kenia Martínez, Geniel Talavera, Juan Alonso

Abstract:

Moringa oleifera is a plant containing many nutrients that are mostly concentrated within the leaves. Commonly, the separation process of these nutrients involves solid-liquid extraction followed by evaporation and drying to obtain a concentrated extract, which is rich in proteins, vitamins, carbohydrates, and other essential nutrients that can be used in the food industry. In this work, three drying methods were used, which involved very different temperature and pressure conditions, to evaluate the effect of each method on the vitamin C content and the antioxidant efficiency of the extracts. Solid-liquid extractions of Moringa leaf (LE) were carried out by employing an ethanol solution (35% v/v) at 50 °C for 2 hours. The resulting extracts were then dried i) in a convective oven (CO) at 100 °C and at an atmospheric pressure of 750 mbar for 8 hours, ii) in a vacuum evaporator (VE) at 50 °C and at 300 mbar for 2 hours, and iii) in a freeze-drier (FD) at -40 °C and at 0.050 mbar for 36 hours. The antioxidant capacity (EC50, mg solids/g DPPH) of the dry solids was calculated by the free radical inhibition method employing DPPH˙ at 517 nm, resulting in a value of 2902.5 ± 14.8 for LE, 3433.1 ± 85.2 for FD, 3980.1 ± 37.2 for VE, and 8123.5 ± 263.3 for CO. The calculated antioxidant efficiency (AE, g DPPH/(mg solids·min)) was 2.920 × 10-5 for LE, 2.884 × 10-5 for FD, 2.512 × 10-5 for VE, and 1.009 × 10-5 for CO. Further, the content of vitamin C (mg/L) determined by HPLC was 59.0 ± 0.3 for LE, 49.7 ± 0.6 for FD, 45.0 ± 0.4 for VE, and 23.6 ± 0.7 for CO. The results indicate that the convective drying preserves vitamin C and antioxidant efficiency to 40% and 34% of the initial value, respectively, while vacuum drying to 76% and 86%, and freeze-drying to 84% and 98%, respectively.

Keywords: antioxidant efficiency, convective drying, freeze-drying, Moringa oleifera, vacuum drying, vitamin C content

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6748 Potassium-Phosphorus-Nitrogen Detection and Spectral Segmentation Analysis Using Polarized Hyperspectral Imagery and Machine Learning

Authors: Nicholas V. Scott, Jack McCarthy

Abstract:

Military, law enforcement, and counter terrorism organizations are often tasked with target detection and image characterization of scenes containing explosive materials in various types of environments where light scattering intensity is high. Mitigation of this photonic noise using classical digital filtration and signal processing can be difficult. This is partially due to the lack of robust image processing methods for photonic noise removal, which strongly influence high resolution target detection and machine learning-based pattern recognition. Such analysis is crucial to the delivery of reliable intelligence. Polarization filters are a possible method for ambient glare reduction by allowing only certain modes of the electromagnetic field to be captured, providing strong scene contrast. An experiment was carried out utilizing a polarization lens attached to a hyperspectral imagery camera for the purpose of exploring the degree to which an imaged polarized scene of potassium, phosphorus, and nitrogen mixture allows for improved target detection and image segmentation. Preliminary imagery results based on the application of machine learning algorithms, including competitive leaky learning and distance metric analysis, to polarized hyperspectral imagery, suggest that polarization filters provide a slight advantage in image segmentation. The results of this work have implications for understanding the presence of explosive material in dry, desert areas where reflective glare is a significant impediment to scene characterization.

Keywords: explosive material, hyperspectral imagery, image segmentation, machine learning, polarization

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6747 Effect of Land Use and Abandonment on Soil Carbon and Nitrogen Depletion by Runoff in Shallow Soils under Semi-Arid Mediterranean Climate

Authors: Mohamed Emran, Giovanni Pardini, Maria Gispert, Mohamed Rashad

Abstract:

Land use and abandonment in semi-arid degraded ecosystems may cause regressive dynamics in vegetation cover affecting organic matter contents, soil nutrients and structural stability, thus reducing soil resistance to erosion. Mediterranean areas are generally subjected to climatic fluctuations, which modify soil conditions and hydrological processes, such as runoff and water infiltration within the upper soil horizons. Low erosion rates occur in very fragile and shallow soils with minor clay content progressively decrease organic carbon C and nitrogen N pools in the upper soil horizons. Seven soils were selected representing variant context of land use and abandonment at the Cap de Creus Peninsula, Catalonia, NE Spain, from recent cultivated vines and olive groves, mid abandoned forests standing under cork and pine trees, pasture to late abandoned Cistus and Erica scrubs. The aim of this work was to study the effect of changes in land use and abandonment on the depletion of soil organic carbon and nitrogen transported by runoff water in shallow soils after natural rainfall events during two years with different rainfall patterns (1st year with low rainfall and 2nd year with high rainfall) by i) monitoring the most significant soil erosion parameters at recorded rainfall events, ii) studying the most relevant soil physical and chemical characteristics on seasonal basis and iii) analysing the seasonal trends of depleted carbon and nitrogen and their interaction with soil surface compaction parameters. Significant seasonal variability was observed in the relevant soil physical and chemical parameters and soil erosion parameters in all soils to establish their evolution under land use and abandonment during two years of different rainfall patterns (214 and 487 mm per year), giving important indications on soil response to rainfall impacts. Erosion rates decreased significantly with the increasing of soil C and N under low and high rainfall. In cultivated soils, C and N depletion increased by 144% and 115%, respectively by 13% increase in erosion rates during the 1st year with respect to the 2nd year. Depleted C and N were proportionally higher in soils under vines and olive with vulnerable soil structure and low soil resilience leading to degradation, altering nutrients cycles and causing adverse impact on environmental quality. Statistical analysis underlined that, during the 1st year, soil surface was less effective in preserving stocks of organic resources leading to higher susceptibility to erosion with consequent C and N depletion. During the 2nd year, higher organic reserve and water storage occurred despite the increasing of C and N loss with an effective contribution from soil surface compaction parameters. The overall estimation during the two years indicated clear differences among soils under vines, olive, cork and pines, suggesting on the one hand, that current cultivation practices are inappropriate and that reforestation with pines may delay the achievement of better soil conditions. On the other hand, the natural succession of vegetation under Cistus, pasture and Erica suggests the recovery of good soil conditions.

Keywords: land abandonment, land use, nutrient's depletion, soil erosion

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6746 An Empirical Study of the Impacts of Big Data on Firm Performance

Authors: Thuan Nguyen

Abstract:

In the present time, data to a data-driven knowledge-based economy is the same as oil to the industrial age hundreds of years ago. Data is everywhere in vast volumes! Big data analytics is expected to help firms not only efficiently improve performance but also completely transform how they should run their business. However, employing the emergent technology successfully is not easy, and assessing the roles of big data in improving firm performance is even much harder. There was a lack of studies that have examined the impacts of big data analytics on organizational performance. This study aimed to fill the gap. The present study suggested using firms’ intellectual capital as a proxy for big data in evaluating its impact on organizational performance. The present study employed the Value Added Intellectual Coefficient method to measure firm intellectual capital, via its three main components: human capital efficiency, structural capital efficiency, and capital employed efficiency, and then used the structural equation modeling technique to model the data and test the models. The financial fundamental and market data of 100 randomly selected publicly listed firms were collected. The results of the tests showed that only human capital efficiency had a significant positive impact on firm profitability, which highlighted the prominent human role in the impact of big data technology.

Keywords: big data, big data analytics, intellectual capital, organizational performance, value added intellectual coefficient

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6745 Checking Energy Efficiency by Simulation Tools: The Case of Algerian Ksourian Models

Authors: Khadidja Rahmani, Nahla Bouaziz

Abstract:

Algeria is known for its rich heritage. It owns an immense historical heritage with a universal reputation. Unfortunately, this wealth is withered because of abundance. This research focuses on the Ksourian model, which constitutes a large portion of this wealth. In fact, the Ksourian model is not just a witness to a great part of history or a vernacular culture, but also it includes a panoply of assets in terms of energetic efficiency. In this context, the purpose of our work is to evaluate the performance of the old techniques which are derived from the Ksourian model , and that using the simulation tools. The proposed method is decomposed in two steps; the first consists of isolate and reintroduce each device into a basic model, then run a simulation series on acquired models. And this in order to test the contribution of each of these dialectal processes. In another scale of development, the second step consists of aggregating all these processes in an aboriginal model, then we restart the simulation, to see what it will give this mosaic on the environmental and energetic plan .The model chosen for this study is one of the ksar units of Knadsa city of Bechar (Algeria). This study does not only show the ingenuity of our ancestors in their know-how, and their adapting power to the aridity of the climate, but also proves that their conceptions subscribe in the current concerns of energy efficiency, and respond to the requirements of sustainable development.

Keywords: dialectal processes, energy efficiency, evaluation, Ksourian model, simulation tools

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6744 A Comprehensive Review of Foam Assisted Water Alternating Gas (FAWAG) Technique: Foam Applications and Mechanisms

Authors: A. Shabib-Asl, M. Abdalla Ayoub Mohammed, A. F. Alta’ee, I. Bin Mohd Saaid, P. Paulo Jose Valentim

Abstract:

In the last few decades, much focus has been placed on enhancing oil recovery from existing fields. This is accomplished by the study and application of various methods. As for recent cases, the study of fluid mobility control and sweep efficiency in gas injection process as well as water alternating gas (WAG) method have demonstrated positive results on oil recovery and thus gained wide interest in petroleum industry. WAG injection application results in an increased oil recovery. Its mechanism consists in reduction of gas oil ratio (GOR). However, there are some problems associated with this which includes poor volumetric sweep efficiency due to its low density and high mobility when compared with oil. This has led to the introduction of foam assisted water alternating gas (FAWAG) technique, which in contrast with WAG injection, acts in improving the sweep efficiency and reducing the gas oil ration therefore maximizing the production rate from the producer wells. This paper presents a comprehensive review of FAWAG process from perspective of Snorre field experience. In addition, some comparative results between FAWAG and the other EOR methods are presented including their setbacks. The main aim is to provide a solid background for future laboratory research and successful field application-extend.

Keywords: GOR, mobility ratio, sweep efficiency, WAG

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6743 The Impact of Efflux Pump Inhibitor on the Activity of Benzosiloxaboroles and Benzoxadiboroles against Gram-Negative Rods

Authors: Agnieszka E. Laudy, Karolina Stępien, Sergiusz Lulinski, Krzysztof Durka, Stefan Tyski

Abstract:

1,3-dihydro-1-hydroxy-2,1-benzoxaborole and its derivatives are a particularly interesting group of synthetic agents and were successfully employed in supramolecular chemistry medicine. The first important compounds, 5-fluoro-1,3-dihydro-1-hydroxy-2,1-benzoxaborole and 5-chloro-1,3-dihydro-1-hydroxy-2,1-benzoxaborole were identified as potent antifungal agents. In contrast, (S)-3-(aminomethyl)-7-(3-hydroxypropoxy)-1-hydroxy-1,3-dihydro-2,1-benzoxaborole hydrochloride is in the second phase of clinical trials as a drug for the treatment of Gram-negative bacterial infections of the Enterobacteriaceae family and Pseudomonas aeruginosa. Equally important and difficult task is to search for compounds active against Gram-negative bacilli, which have multi-drug-resistance efflux pumps actively removing many of the antibiotics from bacterial cells. We have examined whether halogen-substituted benzoxaborole-based derivatives and their analogues possess antibacterial activity and are substrates for multi-drug-resistance efflux pumps. The antibacterial activity of 1,3-dihydro-3-hydroxy-1,1-dimethyl-1,2,3-benzosiloxaborole and 10 halogen-substituted its derivatives, as well as 1,2-phenylenediboronic acid and 3 synthesised fluoro-substituted its analogs, were evaluated. The activity against the reference strains of Gram-positive (n=5) and Gram-negative bacteria (n=10) was screened by the disc-diffusion test (0.4 mg of tested compounds was applied onto paper disc). The minimal inhibitory concentration values and the minimal bactericidal concentration values were estimated according to The Clinical and Laboratory Standards Institute and The European Committee on Antimicrobial Susceptibility Testing recommendations. During the minimal inhibitory concentration values determination with or without phenylalanine-arginine beta-naphthylamide (50 mg/L) efflux pump inhibitor, the concentrations of tested compounds ranged 0.39-400 mg/L in the broth medium supplemented with 1 mM magnesium sulfate. Generally, the studied benzosiloxaboroles and benzoxadiboroles showed a higher activity against Gram-positive cocci than against Gram-negative rods. Moreover, benzosiloxaboroles have the higher activity than benzoxadiboroles compounds. In this study, we demonstrated that substitution (mono-, di- or tetra-) of 1,3-dihydro-3-hydroxy-1,1-dimethyl-1,2,3-benzosiloxaborole with halogen groups resulted in an increase in antimicrobial activity as compared to the parent substance. Interestingly, the 6,7-dichloro-substituted parent substance was found to be the most potent against Gram-positive cocci: Staphylococcus sp. (minimal inhibitory concentration 6.25 mg/L) and Enterococcus sp. (minimal inhibitory concentration 25 mg/L). On the other hand, mono- and dichloro-substituted compounds were the most actively removed by efflux pumps present in Gram-negative bacteria mainly from Enterobacteriaceae family. In the presence of efflux pump inhibitor the minimal inhibitory concentration values of chloro-substituted benzosiloxaboroles decreased from 400 mg/L to 3.12 mg/L. Of note, the highest increase in bacterial susceptibility to tested compounds in the presence of phenylalanine-arginine beta-naphthylamide was observed for 6-chloro-, 6,7-dichloro- and 6,7-difluoro-substituted benzosiloxaboroles. In the case of Escherichia coli, Enterobacter cloacae and P. aeruginosa strains at least a 32-fold decrease in the minimal inhibitory concentration values of these agents were observed. These data demonstrate structure-activity relationships of the tested derivatives and highlight the need for further search for benzoxaboroles and related compounds with significant antimicrobial properties. Moreover, the influence of phenylalanine-arginine beta-naphthylamide on the susceptibility of Gram-negative rods to studied benzosiloxaboroles indicate that some tested agents are substrates for efflux pumps in Gram-negative rods.

Keywords: antibacterial activity, benzosiloxaboroles, efflux pumps, phenylalanine-arginine beta-naphthylamide

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6742 Identification of Potent and Selective SIRT7 Anti-Cancer Inhibitor via Structure-Based Virtual Screening and Molecular Dynamics Simulation

Authors: Md. Fazlul Karim, Ashik Sharfaraz, Aysha Ferdoushi

Abstract:

Background: Computational medicinal chemistry approaches are used for designing and identifying new drug-like molecules, predicting properties and pharmacological activities, and optimizing lead compounds in drug development. SIRT7, a nicotinamide adenine dinucleotide (NAD+)-dependent deacylase which regulates aging, is an emerging target for cancer therapy with mounting evidence that SIRT7 downregulation plays important roles in reversing cancer phenotypes and suppressing tumor growth. Activation or altered expression of SIRT7 is associated with the progression and invasion of various cancers, including liver, breast, gastric, prostate, and non-small cell lung cancer. Objectives: The goal of this work was to identify potent and selective bioactive candidate inhibitors of SIRT7 by in silico screening of small molecule compounds obtained from Nigella sativa (N. sativa). Methods: SIRT7 structure was retrieved from The Research Collaboratory for Structural Bioinformatics Protein Data Bank (RCSB PDB), and its active site was identified using CASTp and metaPocket. Molecular docking simulation was performed with PyRx 0.8 virtual screening software. Drug-likeness properties were tested using SwissADME and pkCSM. In silico toxicity was evaluated by Osiris Property Explorer. Bioactivity was predicted by Molinspiration software. Antitumor activity was screened for Prediction of Activity Spectra for Substances (PASS) using Way2Drug web server. Molecular dynamics (MD) simulation was carried out by Desmond v3.6 package. Results: A total of 159 bioactive compounds from the N. Sativa were screened against the SIRT7 enzyme. Five bioactive compounds: chrysin (CID:5281607), pinocembrin (CID:68071), nigellidine (CID:136828302), nigellicine (CID:11402337), and epicatechin (CID:72276) were identified as potent SIRT7 anti-cancer candidates after docking score evaluation and applying Lipinski's Rule of Five. Finally, MD simulation identified Chrysin as the top SIRT7 anti-cancer candidate molecule. Conclusion: Chrysin, which shows a potential inhibitory effect against SIRT7, can act as a possible anti-cancer drug candidate. This inhibitor warrants further evaluation to check its pharmacokinetics and pharmacodynamics properties both in vitro and in vivo.

Keywords: SIRT7, antitumor, molecular docking, molecular dynamics simulation

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6741 Development of Ketorolac Tromethamine Encapsulated Stealth Liposomes: Pharmacokinetics and Bio Distribution

Authors: Yasmin Begum Mohammed

Abstract:

Ketorolac tromethamine (KTM) is a non-steroidal anti-inflammatory drug with a potent analgesic and anti-inflammatory activity due to prostaglandin related inhibitory effect of drug. It is a non-selective cyclo-oxygenase inhibitor. The drug is currently used orally and intramuscularly in multiple divided doses, clinically for the management arthritis, cancer pain, post-surgical pain, and in the treatment of migraine pain. KTM has short biological half-life of 4 to 6 hours, which necessitates frequent dosing to retain the action. The frequent occurrence of gastrointestinal bleeding, perforation, peptic ulceration, and renal failure lead to the development of other drug delivery strategies for the appropriate delivery of KTM. The ideal solution would be to target the drug only to the cells or tissues affected by the disease. Drug targeting could be achieved effectively by liposomes that are biocompatible and biodegradable. The aim of the study was to develop a parenteral liposome formulation of KTM with improved efficacy while reducing side effects by targeting the inflammation due to arthritis. PEG-anchored (stealth) and non-PEG-anchored liposomes were prepared by thin film hydration technique followed by extrusion cycle and characterized for in vitro and in vivo. Stealth liposomes (SLs) exhibited increase in percent encapsulation efficiency (94%) and 52% percent of drug retention during release studies in 24 h with good stability for a period of 1 month at -20°C and 4°C. SLs showed about maximum 55% of edema inhibition with significant analgesic effect. SLs produced marked differences over those of non-SL formulations with an increase in area under plasma concentration time curve, t₁/₂, mean residence time, and reduced clearance. 0.3% of the drug was detected in arthritic induced paw with significantly reduced drug localization in liver, spleen, and kidney for SLs when compared to other conventional liposomes. Thus SLs help to increase the therapeutic efficacy of KTM by increasing the targeting potential at the inflammatory region.

Keywords: biodistribution, ketorolac tromethamine, stealth liposomes, thin film hydration technique

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6740 Study on the Retaining Sleeve Structure for the Reduction of Eddy Current in SPMSM

Authors: Hyun-Woo Jun, In-Gun Kim, Hyun Seok Hong, Dong-Woo Kang, Ju Lee

Abstract:

In high-speed SPMSM design, the rotor-retaining sleeve is inserted into rotor to prevent permanent magnet’s damage. It is quite efficient way considering manufacturability, but the sleeve becomes major source of ohm loss in high-speed operation. In this paper, the high-speed motor for turbo-blower at the rating of 100kW was introduced. To improve its efficiency, the retaining sleeve’s optimal design was needed. Within the range of satisfies the mechanical safety, sleeve’s some design variables have been changed. The effect of changing design variables of the sleeve was studied. This paper presents the optimized sleeve’s advantages in electrical efficiency from the result of electromagnetic FEA (finite element analysis) software. Finally, it suggests the optimal sleeve design to reduce eddy current loss, which is related to motor shape.

Keywords: SPMSM, sleeve, eddy current, high efficiency

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6739 Binderless Naturally-extracted Metal-free Electrocatalyst for Efficient NOₓ Reduction

Authors: Hafiz Muhammad Adeel Sharif, Tian Li, Changping Li

Abstract:

Recently, the emission of nitrogen-sulphur oxides (NOₓ, SO₂) has become a global issue and causing serious threats to health and the environment. Catalytic reduction of NOx and SOₓ gases into friendly gases is considered one of the best approaches. However, regeneration of the catalyst, higher bond-dissociation energy for NOx, i.e., 150.7 kcal/mol, escape of intermediate gas (N₂O, a greenhouse gas) with treated flue-gas, and limited activity of catalyst remains a great challenge. Here, a cheap, binderless naturally-extracted bass-wood thin carbon electrode (TCE) is presented, which shows excellent catalytic activity towards NOx reduction. The bass-wood carbonization at 900 ℃ followed by thermal activation in the presence of CO2 gas at 750 ℃. The thermal activation resulted in an increase in epoxy groups on the surface of the TCE and enhancement in the surface area as well as the degree of graphitization. The TCE unique 3D strongly inter-connected network through hierarchical micro/meso/macro pores that allow large electrode/electrolyte interface. Owing to these characteristics, the TCE exhibited excellent catalytic efficiency towards NOx (~83.3%) under ambient conditions and enhanced catalytic response under pH and sulphite exposure as well as excellent stability up to 168 hours. Moreover, a temperature-dependent activity trend was found where the highest catalytic activity was achieved at 80 ℃, beyond which the electrolyte became evaporative and resulted in a performance decrease. The designed electrocatalyst showed great potential for effective NOx-reduction, which is highly cost-effective, green, and sustainable.

Keywords: electrocatalyst, NOx-reduction, bass-wood electrode, integrated wet-scrubbing, sustainable

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6738 Method of Estimating Absolute Entropy of Municipal Solid Waste

Authors: Francis Chinweuba Eboh, Peter Ahlström, Tobias Richards

Abstract:

Entropy, as an outcome of the second law of thermodynamics, measures the level of irreversibility associated with any process. The identification and reduction of irreversibility in the energy conversion process helps to improve the efficiency of the system. The entropy of pure substances known as absolute entropy is determined at an absolute reference point and is useful in the thermodynamic analysis of chemical reactions; however, municipal solid waste (MSW) is a structurally complicated material with unknown absolute entropy. In this work, an empirical model to calculate the absolute entropy of MSW based on the content of carbon, hydrogen, oxygen, nitrogen, sulphur, and chlorine on a dry ash free basis (daf) is presented. The proposed model was derived from 117 relevant organic substances which represent the main constituents in MSW with known standard entropies using statistical analysis. The substances were divided into different waste fractions; namely, food, wood/paper, textiles/rubber and plastics waste and the standard entropies of each waste fraction and for the complete mixture were calculated. The correlation of the standard entropy of the complete waste mixture derived was found to be somsw= 0.0101C + 0.0630H + 0.0106O + 0.0108N + 0.0155S + 0.0084Cl (kJ.K-1.kg) and the present correlation can be used for estimating the absolute entropy of MSW by using the elemental compositions of the fuel within the range of 10.3%  C 95.1%, 0.0%  H  14.3%, 0.0%  O  71.1%, 0.0  N  66.7%, 0.0%  S  42.1%, 0.0%  Cl  89.7%. The model is also applicable for the efficient modelling of a combustion system in a waste-to-energy plant.

Keywords: absolute entropy, irreversibility, municipal solid waste, waste-to-energy

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6737 Insight on Passive Design for Energy Efficiency in Commercial Building for Hot and Humid Climate

Authors: Aravind J.

Abstract:

Passive design can be referred to a way of designing buildings that takes advantage of the prevailing climate and natural energy resources. Which will be a key to reduce the increasing energy usage in commercial buildings. Most of the small scale commercial buildings made are merely a thermal mass inbuilt with active systems to bring lively conditions. By bringing the passive design strategies for energy efficiency in commercial buildings will reduce the usage of active systems. Thus the energy usage can be controlled through analysis of daylighting and improved living conditions in the indoor spaces by using passive techniques. And comparative study on different passive design systems and conventional methods will be approached for commercial buildings in hot and humid region. Possible effects of existing risks implied with solution for those problems is also a part of the paper. The result will be carried on with the design programme to prove the workability of the strategies.

Keywords: passive design, energy efficiency, commercial buildings, hot and humid climate

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6736 Occurrence of Illicit Drugs in Aqueous Environment and Removal Efficiency of Wastewater Treatment Plants

Authors: Meena K. Yadav, Rupak Aryal, Michael D. Short, Ben Van Den Akker, Christopher P. Saint, Cobus Gerber

Abstract:

Illicit drugs are considered as emerging contaminants of concern that have become an interesting issue for the scientific community from last few years due to their existence in the water environment. A number of the literature has revealed their occurrence in the environment. This is mainly due to the fact that some drugs are partially removed during wastewater treatment processes, and remaining being able to enter the environment and contaminate surface and groundwater and subsequently, drinking water. Therefore, this paper evaluates the occurrence of key illicit drugs in wastewater (influent and effluent) samples in 4 wastewater treatment plants across Adelaide, South Australia over a 1 year period. This paper also compares the efficiency of wastewater treatment plants adopting different technologies in the removal of selected illicit drugs, especially in the context of which technology has higher removal rates. The influent and effluent samples were analysed using Liquid Chromatography tandem Mass Spectrometry (LC-MS/MS). The levels of drugs detected were in the range of mg/L – ng/L in effluent samples; thus emphasising the influence on water quality of receiving water bodies and the significance of removal efficiency of WWTPs(Wastewater Treatment Plants). The results show that the drugs responded differently in the removal depending on the treatment processes used by the WWTPs.

Keywords: illicit drugs, removal efficiency, treatment technology, wastewater

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6735 Adsorption of NO and NH3 in MFI and H-ZSM5: Monte Carlo Simulation

Authors: Z. Jamalzadeh, A. Niaei, H. Erfannia

Abstract:

Due to developing industries, the emission of pollutants such as NOx, SOx, and CO2 are rapidly increased. Generally, NOx is attributed to the mono nitrogen oxides of NO and NO2 that is one of the most important atmospheric contaminants. Hence, controlling the emission of nitrogen oxides is environmentally urgent. Selective catalytic reduction of NOx is one of the most common techniques for NOx removal in which zeolites have wide application due to their high performance. In zeolitic processes, the catalytic reaction occurs mostly in the pores. Therefore, investigation of the adsorption phenomena of the molecules in order to gain an insight and understand the catalytic cycle is of important. Hence, in current study, benefiting from molecular simulations, the adsorption phenomena in the nanocatalysts of SCR of NOx process was investigated in order to get a good insight of the catalysts’ behavior. The effect of cation addition to the support in the catalysts’ behavior through adsorption step was explored by Mont Carlo (MC) using Materials Studio Package. Simulation time of 1 Ns accompanying 1 fs time step, COMPASS27 Force Field and the cut off radios of 12.5 Ȧ was applied for performed runs. It was observed that the adsorption capacity increases in the presence of cations. The sorption isotherms demonstrated the behavior of type I isotherm categories and sorption capacity diminished with increase in temperature whereas an increase was observed at high pressures. Besides, NO sorption showed higher sorption capacity than NH3 in H–ZSM5. In this respect, the energy distributions signified that the molecules could adsorb in just one sorption site at the catalyst and the sorption energy of NO was stronger than the NH3 in H-ZSM5. Furthermore, the isosteric heat of sorption data showed nearly same values for the molecules; however, it indicated stronger interactions of NO molecules with H-ZSM5 zeolite compared to the isosteric heat of NH3 which was low in value.

Keywords: Monte Carlo simulation, adsorption, NOx, ZSM5

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6734 Study of Clutch Cable Architecture and Its Influence in Efficiency of Mechanical Cable Release System

Authors: M. Devamanalan, K. Pothiraj, M. Sudhan

Abstract:

In competitive market like India, there is a high demand on the equal contribution on performance and its durability aspect of any system. In General vehicle has multiple sub-systems such as powertrain, BIW, Brakes, Actuations, Suspension and Seats etc., To withstand the market challenges, the contribution of each sub-system is very vital. The malfunction of any one sub system will directly have an impact on the performance of the major system which lead to dis-satisfaction to the end user. The Powertrain system consists of several sub-systems in which clutch is one of the prime sub-systems in MT vehicles which assist for smoother gear shifts with proper clutch dis-engagement and engagement. In general, most of the vehicles will have a mechanical or semi or full hydraulic clutch release system, whereas in small Commercial Vehicles (SCV) the majorly used clutch release system is mechanical cable release system due to its lesser cost and functional requirements. The major bottle neck in the cable type clutch release system is increase in pedal effort due to hysteresis increase and Gear shifting hard due to efficiency loss / cable slackness over the mileage accumulation of the vehicle. This study is to mainly focus on how the efficiency and hysteresis change over the mileage of the vehicle occurs because of the design architecture of outer and inner cable. The study involves several cable design validation results from vehicle level and rig level through the defined cable routing and test procedures. Results are compared to evaluate the suitable cable design architecture based on better efficiency and lower hysteresis parameters at initial and end of the validation.

Keywords: clutch, clutch cable, efficiency, architecture, cable routing

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6733 On Board Measurement of Real Exhaust Emission of Light-Duty Vehicles in Algeria

Authors: R. Kerbachi, S. Chikhi, M. Boughedaoui

Abstract:

The study presents an analysis of the Algerian vehicle fleet and resultant emissions. The emission measurement of air pollutants emitted by road transportation (CO, THC, NOX and CO2) was conducted on 17 light duty vehicles in real traffic. This sample is representative of the Algerian light vehicles in terms of fuel quality (gasoline, diesel and liquefied petroleum gas) and the technology quality (injection system and emission control). The experimental measurement methodology of unit emission of vehicles in real traffic situation is based on the use of the mini-Constant Volume Sampler for gas sampling and a set of gas analyzers for CO2, CO, NOx and THC, with an instrumentation to measure kinematics, gas temperature and pressure. The apparatus is also equipped with data logging instrument and data transfer. The results were compared with the database of the European light vehicles (Artemis). It was shown that the technological injection liquefied petroleum gas (LPG) has significant impact on air pollutants emission. Therefore, with the exception of nitrogen oxide compounds, uncatalyzed LPG vehicles are more effective in reducing emissions unit of air pollutants compared to uncatalyzed gasoline vehicles. LPG performance seems to be lower under real driving conditions than expected on chassis dynamometer. On the other hand, the results show that uncatalyzed gasoline vehicles emit high levels of carbon monoxide, and nitrogen oxides. Overall, and in the absence of standards in Algeria, unit emissions are much higher than Euro 3. The enforcement of pollutant emission standard in developing countries is an important step towards introducing cleaner technology and reducing vehicular emissions.

Keywords: on-board measurements of unit emissions of CO, HC, NOx and CO2, light vehicles, mini-CVS, LPG-fuel, artemis, Algeria

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6732 Identification, Synthesis, and Biological Evaluation of the Major Human Metabolite of NLRP3 Inflammasome Inhibitor MCC950

Authors: Manohar Salla, Mark S. Butler, Ruby Pelingon, Geraldine Kaeslin, Daniel E. Croker, Janet C. Reid, Jong Min Baek, Paul V. Bernhardt, Elizabeth M. J. Gillam, Matthew A. Cooper, Avril A. B. Robertson

Abstract:

MCC950 is a potent and selective inhibitor of the NOD-like receptor pyrin domain-containing protein 3 (NLRP3) inflammasome that shows early promise for treatment of inflammatory diseases. The identification of major metabolites of lead molecule is an important step during drug development process. It provides an information about the metabolically labile sites in the molecule and thereby helping medicinal chemists to design metabolically stable molecules. To identify major metabolites of MCC950, the compound was incubated with human liver microsomes and subsequent analysis by (+)- and (−)-QTOF-ESI-MS/MS revealed a major metabolite formed due to hydroxylation on 1,2,3,5,6,7-hexahydro-s-indacene moiety of MCC950. This major metabolite can lose two water molecules and three possible regioisomers were synthesized. Co-elution of major metabolite with each of the synthesized compounds using HPLC-ESI-SRM-MS/MS revealed the structure of the metabolite (±) N-((1-hydroxy-1,2,3,5,6,7-hexahydro-s-indacen-4-yl)carbamoyl)-4-(2-hydroxypropan-2-yl)furan-2-sulfonamide. Subsequent synthesis of individual enantiomers and coelution in HPLC-ESI-SRM-MS/MS using a chiral column revealed the metabolite was R-(+)- N-((1-hydroxy-1,2,3,5,6,7-hexahydro-s-indacen-4-yl)carbamoyl)-4-(2-hydroxypropan-2-yl)furan-2-sulfonamide. To study the possible cytochrome P450 enzyme(s) responsible for the formation of major metabolite, MCC950 was incubated with a panel of cytochrome P450 enzymes. The result indicated that CYP1A2, CYP2A6, CYP2B6, CYP2C9, CYP2C18, CYP2C19, CYP2J2 and CYP3A4 are most likely responsible for the formation of the major metabolite. The biological activity of the major metabolite and the other synthesized regioisomers was also investigated by screening for for NLRP3 inflammasome inhibitory activity and cytotoxicity. The major metabolite had 170-fold less inhibitory activity (IC50-1238 nM) than MCC950 (IC50-7.5 nM). Interestingly, one regioisomer had shown nanomolar inhibitory activity (IC50-232 nM). However, no evidence of cytotoxicity was observed with any of these synthesized compounds when tested in human embryonic kidney 293 cells (HEK293) and human liver hepatocellular carcinoma G2 cells (HepG2). These key findings give an insight into the SAR of the hexahydroindacene moiety of MCC950 and reveal a metabolic soft spot which could be blocked by chemical modification.

Keywords: Cytochrome P450, inflammasome, MCC950, metabolite, microsome, NLRP3

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6731 DPAGT1 Inhibitors: Discovery of Anti-Metastatic Drugs

Authors: Michio Kurosu

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Alterations in glycosylation not only directly impact cell growth and survival but also facilitate tumor-induced immunomodulation and eventual metastasis. Identification of cell type-specific glycoconjugates (tumor markers) has led to the discovery of new assay systems for certain cancers via immunodetection reagents. N- and O-linked glycans are the most abundant forms of glycoproteins. Recent studies of cancer immunotherapy are based on the immunogenicity of truncated O-glycan chains (e.g., Tn, sTn, T, and sLea/x). The prevalence of N-linked glycan changes in the development of tumor cells is known; however, therapeutic antibodies against N-glycans have not yet been developed. This is due to the lack of specificity of N-linked glycans between normal/healthy and cancer cells. Abnormal branching of N-linked glycans has been observed, particularly in solid cancer cells. While the discovery of drug-like glycosyltransferase inhibitors that block the biosynthesis of specific branching has a very low likelihood of success, altered glycosylation levels can be exploited by suppressing N-glycan biosynthesis through the inhibition of dolichyl-phosphate N-acetylglucosaminephosphotransferase1 (DPAGT1) activity. Inhibition of DPAGT1 function leads to changes of O-glycosylation on proteins associated with mitochondria and zinc finger binding proteins (indirect effects). On the basis of dynamic crosstalk between DPAGT1 and Snail/Slung/ZEB1 (a family of transcription factors that promote the repression of the adhesion molecules), we have developed pharmacologically acceptable selective DPAGT1 inhibitors. Tunicamycin kills a wide range of cancer and healthy cells in a non-selective manner. In sharp contrast, our DPAGT1 inhibitors display strong cytostatic effects against 16 solid cancers, which require the overexpression of DPAGT1 in their progression but do not affect the cell viability of healthy cells. The identified DPAGT1 inhibitors possess impressive anti-metastatic ability in various solid cancer cell lines and induce their mitochondrial structural changes, resulting in apoptosis. A prototype DPAGT1 inhibitor, APPB has already been proven to shrink solid tumors (e.g., pancreatic cancers, triple-negative breast cancers) in vivo while suppressing metastases and has strong synergistic effects when combined with current cytotoxic drugs (e.g., paclitaxel). At this conference, our discovery of selective DPAGT1 inhibitors with drug-like properties and proof-of-pharmaceutical concept studies of a novel DPAGT1 inhibitor are presented.

Keywords: DPAGT1 inhibitors, anti-metastatic drugs, natural product based drug designs, cytostatic effects

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