Search results for: stagnation properties
Commenced in January 2007
Frequency: Monthly
Edition: International
Paper Count: 9081

Search results for: stagnation properties

1881 Multilayer Thermal Screens for Greenhouse Insulation

Authors: Clara Shenderey, Helena Vitoshkin, Mordechai Barak, Avraham Arbel

Abstract:

Greenhouse cultivation is an energy-intensive process due to the high demands on cooling or heating according to external climatic conditions, which could be extreme in the summer or winter seasons. The thermal radiation rate inside a greenhouse depends mainly on the type of covering material and greenhouse construction. Using additional thermal screens under a greenhouse covering combined with a dehumidification system improves the insulation and could be cost-effective. Greenhouse covering material usually contains protective ultraviolet (UV) radiation additives to prevent the film wear, insect harm, and crop diseases. This paper investigates the overall heat transfer coefficient, or U-value, for greenhouse polyethylene covering contains UV-additives and glass covering with or without a thermal screen supplement. The hot-box method was employed to evaluate overall heat transfer coefficients experimentally as a function of the type and number of the thermal screens. The results show that the overall heat transfer coefficient decreases with increasing the number of thermal screens as a hyperbolic function. The overall heat transfer coefficient highly depends on the ability of the material to reflect thermal radiation. Using a greenhouse covering, i.e., polyethylene films or glass, in combination with high reflective thermal screens, i.e., containing about 98% of aluminum stripes or aluminum foil, the U-value reduces by 61%-89% in the first case, whereas by 70%-92% in the second case, depending on the number of the thermal screen. Using thermal screens made from low reflective materials may reduce the U-value by 30%-57%. The heat transfer coefficient is an indicator of the thermal insulation properties of the materials, which allows farmers to make decisions on the use of appropriate thermal screens depending on the external and internal climate conditions in a greenhouse.

Keywords: energy-saving thermal screen, greenhouse cover material, heat transfer coefficient, hot box

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1880 Peculiarities of Internal Friction and Shear Modulus in 60Co γ-Rays Irradiated Monocrystalline SiGe Alloys

Authors: I. Kurashvili, G. Darsavelidze, T. Kimeridze, G. Chubinidze, I. Tabatadze

Abstract:

At present, a number of modern semiconductor devices based on SiGe alloys have been created in which the latest achievements of high technologies are used. These devices might cause significant changes to networking, computing, and space technology. In the nearest future new materials based on SiGe will be able to restrict the A3B5 and Si technologies and firmly establish themselves in medium frequency electronics. Effective realization of these prospects requires the solution of prediction and controlling of structural state and dynamical physical –mechanical properties of new SiGe materials. Based on these circumstances, a complex investigation of structural defects and structural-sensitive dynamic mechanical characteristics of SiGe alloys under different external impacts (deformation, radiation, thermal cycling) acquires great importance. Internal friction (IF) and shear modulus temperature and amplitude dependences of the monocrystalline boron-doped Si1-xGex(x≤0.05) alloys grown by Czochralski technique is studied in initial and 60Co gamma-irradiated states. In the initial samples, a set of dislocation origin relaxation processes and accompanying modulus defects are revealed in a temperature interval of 400-800 ⁰C. It is shown that after gamma-irradiation intensity of relaxation internal friction in the vicinity of 280 ⁰C increases and simultaneously activation parameters of high temperature relaxation processes reveal clear rising. It is proposed that these changes of dynamical mechanical characteristics might be caused by a decrease of the dislocation mobility in the Cottrell atmosphere enriched by the radiation defects.

Keywords: internal friction, shear modulus, gamma-irradiation, SiGe alloys

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1879 Synthesis of Pendent Compartmental Ligand Derived from Polymethacrylate of 3-Formylsalicylic Acid Schiff Base and Its Application Studies

Authors: Dhivya Arumugam, Kaliyappan Thananjeyan

Abstract:

The monomer of (3-((4-(methacryloyloxy)phenylimino)methyl)-2-hydroxybenzoic acid) schiff base polymer was prepared by reacting methacryloyl chloride with imine compound derived from 3-formylsalisylic acid and 4- aminophenol. The monomer was polymerized in DMF at 70oC using benzoyl peroxide as free radical initiator. Polymer metal complex was obtained in DMF solution of polymer with aqueous solution of metal ions. The polymer and the polymer metal complex were characterized by elemental analysis and spectral studies. The elemental analysis data suggest that the metal to ligand ratio is 1:1 and hence, it acts as a binucleating compartmental ligand. The IR spectral data of these complexes suggest that the metals are coordinated through nitrogen of the imine group, the oxygen of carboxylate ion and the oxygen of the phenolic –OH group which also acts as the bridging ligand. The electronic spectra and magnetic moments of the polychelates shows that octahedral and square planar structure for Ni(II) and Cu(II) complexes respectively. X-ray diffraction studies revealed that polychelates are highly crystalline. The thermal and electrical properties, catalytic activity, structure property relationships are discussed. Further the synthesized polymer was used for metal uptake studies from waste water, which is one of the effective waste water treatment strategies. And also, the polymers and polychelates were investigated for antimicrobial activity with various microorganisms by using agar well diffusion method and the results have been discussed.

Keywords: acyclic compartmental ligands, binucleating ligand, 3-formylsalicylic acid, free radical polymerization, polluting ions, polychelate

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1878 Comparing Field Displacement History with Numerical Results to Estimate Geotechnical Parameters: Case Study of Arash-Esfandiar-Niayesh under Passing Tunnel, 2.5 Traffic Lane Tunnel, Tehran, Iran

Authors: A. Golshani, M. Gharizade Varnusefaderani, S. Majidian

Abstract:

Underground structures are of those structures that have uncertainty in design procedures. That is due to the complexity of soil condition around. Under passing tunnels are also such affected structures. Despite geotechnical site investigations, lots of uncertainties exist in soil properties due to unknown events. As results, it possibly causes conflicting settlements in numerical analysis with recorded values in the project. This paper aims to report a case study on a specific under passing tunnel constructed by New Austrian Tunnelling Method in Iran. The intended tunnel has an overburden of about 11.3m, the height of 12.2m and, the width of 14.4m with 2.5 traffic lane. The numerical modeling was developed by a 2D finite element program (PLAXIS Version 8). Comparing displacement histories at the ground surface during the entire installation of initial lining, the estimated surface settlement was about four times the field recorded one, which indicates that some local unknown events affect that value. Also, the displacement ratios were in a big difference between the numerical and field data. Consequently, running several numerical back analyses using laboratory and field tests data, the geotechnical parameters were accurately revised to match with the obtained monitoring data. Finally, it was found that usually the values of soil parameters are conservatively low-estimated up to 40 percent by typical engineering judgment. Additionally, it could be attributed to inappropriate constitutive models applied for the specific soil condition.

Keywords: NATM, surface displacement history, numerical back-analysis, geotechnical parameters

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1877 Numerical Calculation and Analysis of Fine Echo Characteristics of Underwater Hemispherical Cylindrical Shell

Authors: Hongjian Jia

Abstract:

A finite-length cylindrical shell with a spherical cap is a typical engineering approximation model of actual underwater targets. The research on the omni-directional acoustic scattering characteristics of this target model can provide a favorable basis for the detection and identification of actual underwater targets. The elastic resonance characteristics of the target are the results of the comprehensive effect of the target length, shell-thickness ratio and materials. Under the conditions of different materials and geometric dimensions, the coincidence resonance characteristics of the target have obvious differences. Aiming at this problem, this paper obtains the omni-directional acoustic scattering field of the underwater hemispherical cylindrical shell by numerical calculation and studies the influence of target geometric parameters (length, shell-thickness ratio) and material parameters on the coincidence resonance characteristics of the target in turn. The study found that the formant interval is not a stable value and changes with the incident angle. Among them, the formant interval is less affected by the target length and shell-thickness ratio and is significantly affected by the material properties, which is an effective feature for classifying and identifying targets of different materials. The quadratic polynomial is utilized to fully fit the change relationship between the formant interval and the angle. The results show that the three fitting coefficients of the stainless steel and aluminum targets are significantly different, which can be used as an effective feature parameter to characterize the target materials.

Keywords: hemispherical cylindrical shell;, fine echo characteristics;, geometric and material parameters;, formant interval

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1876 Air Pollution: The Journey from Single Particle Characterization to in vitro Fate

Authors: S. Potgieter-Vermaak, N. Bain, A. Brown, K. Shaw

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It is well-known from public news media that air pollution is a health hazard and is responsible for early deaths. The quantification of the relationship between air quality and health is a probing question not easily answered. It is known that airborne particulate matter (APM) <2.5µm deposits in the tracheal and alveoli zones and our research probes the possibility of quantifying pulmonary injury by linking reactive oxygen species (ROS) in these particles to DNA damage. Currently, APM mass concentration is linked to early deaths and limited studies probe the influence of other properties on human health. To predict the full extent and type of impact, particles need to be characterised for chemical composition and structure. APMs are routinely analysed for their bulk composition, but of late analysis on a micro level probing single particle character, using micro-analytical techniques, are considered. The latter, single particle analysis (SPA), permits one to obtain detailed information on chemical character from nano- to micron-sized particles. This paper aims to provide a snapshot of studies using data obtained from chemical characterisation and its link with in-vitro studies to inform on personal health risks. For this purpose, two studies will be compared, namely, the bioaccessibility of the inhalable fraction of urban road dust versus total suspended solids (TSP) collected in the same urban environment. The significant influence of metals such as Cu and Fe in TSP on DNA damage is illustrated. The speciation of Hg (determined by SPA) in different urban environments proved to dictate its bioaccessibility in artificial lung fluids rather than its concentration.

Keywords: air pollution, human health, in-vitro studies, particulate matter

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1875 Translation and Validation of the Pediatric Quality of Life Inventory for Children in Pakistani Context

Authors: Nazia Mustafa, Aneela Maqsood

Abstract:

Pediatric Quality of Life Inventory is the most widely used instrument for assessing children and adolescent health-related quality of life and has shown excellent markers of reliability and validity. The current study was carried out with the objectives of translation and cross-language validation along with the determination of factor Structure and psychometric properties of the Urdu version. It was administered on 154 Primary School Children with age range 10 to12 years (M= 10.86, S.D = 0.62); including boys (n=92) and girls (n = 62). The sample was recruited from two randomly selected schools from the Rawalpindi district of Pakistan. Results of the pilot phase revealed that the instrument had good reliability (Urdu Version α = 0.798; English Version α = 0.795) as well as test-retest correlation coefficients over a period of 15 days (r = 0.85). Exploratory factor analysis (EFA) resulted in three factorial structures; Social/School Functioning (k = 8), Psychological Functioning (k = 7) and Physical Functioning (k = 6) considered suitable for our sample instead of four factors. Bartlett's test of sphericity showed inter-correlation between variables. However, factor loadings for items 22 and 23 of the School Functioning subscale were problematic. The model was fit to the data after their removal with Cronbach’s Alpha Reliability coefficient of the scale (k = 21) as 0.87 and for subscales as 0.75, 0.77 and 0.73 for Social/School Scale, Psychological subscale and Physical subscale, respectively. These results supported the feasibility and reliability of the Urdu version of the Pediatric Quality of Life Inventory as a reliable and effective tool for the measurement of quality of life among Pediatrics Pakistani population.

Keywords: primary school children, paediatric quality of life, exploratory factor analysis, Pakistan

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1874 Comparison of Physicochemical Properties of Catfish Myofibrillar and Sarcoplasmic Protein Hydrolysates and Characterization of Their Bioactive Peptides

Authors: Leila Najafian

Abstract:

Sarcoplasmic protein hydrolysates (SPHs) and myofibrillar protein hydrolysates (MPHs) from patin (Pangasius sutchi) were produced using two types of proteases: Papain and Alcalase. 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) diammonium salt (ABTS) radical scavenging activities and metal chelating activity assays for antioxidant activities were carried out on the SPHs and MPHs. The hydrolysates were isolated and purified by ultrafiltration, gel filtration and reverse phase high-performance liquid chromatography (RP-HPLC) and liquid chromatography with tandem mass spectrometry detection (LC-MS/MS) was used in identifying peptide sequences. The results showed that when the DH of MPHs increased, the protein solubility increased, while the highest amount of the protein solubility of SPHs was after 60 min incubation. The effect of DH on antioxidant activities of SPHs and MPHs was investigated. Among the hydrolysates, papain-MPH and Alcalase-SPH, which had the highest antioxidant activities, were purified. The potent fractions obtained from RP-HPLC of sarcoplasmic (SI 3 fraction) and myofibrillar (MI 4 fraction) hydrolysates showed the highest DPPH radical scavenging activity. The FVNQPYLLYSVHMK peptide for MPH and the LVVDIPAALQHA peptide for SPH exhibited the highest antioxidant activity. The presence of hydrophobic and hydrophilic amino acids, namely leucine (L), valine (V), phenylalanine (F), histidine (H) and proline (P), in the peptide sequences of SPH and MPH are believed to contribute to high antioxidant activity. Hence, SPH and MPH from patin have the potential as a natural functional ingredient in food and pharmaceutical industry.

Keywords: patin (Pangasius sutchi), protein hydrolysates, antioxidative peptides, mass spectrometry

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1873 Lipid-Chitosan Hybrid Nanoparticles for Controlled Delivery of Cisplatin

Authors: Muhammad Muzamil Khan, Asadullah Madni, Nina Filipczek, Jiayi Pan, Nayab Tahir, Hassan Shah, Vladimir Torchilin

Abstract:

Lipid-polymer hybrid nanoparticles (LPHNP) are delivery systems for controlled drug delivery at tumor sites. The superior biocompatible properties of lipid and structural advantages of polymer can be obtained via this system for controlled drug delivery. In the present study, cisplatin-loaded lipid-chitosan hybrid nanoparticles were formulated by the single step ionic gelation method based on ionic interaction of positively charged chitosan and negatively charged lipid. Formulations with various chitosan to lipid ratio were investigated to obtain the optimal particle size, encapsulation efficiency, and controlled release pattern. Transmission electron microscope and dynamic light scattering analysis demonstrated a size range of 181-245 nm and a zeta potential range of 20-30 mV. Compatibility among the components and the stability of formulation were demonstrated with FTIR analysis and thermal studies, respectively. The therapeutic efficacy and cellular interaction of cisplatin-loaded LPHNP were investigated using in vitro cell-based assays in A2780/ADR ovarian carcinoma cell line. Additionally, the cisplatin loaded LPHNP exhibited a low toxicity profile in rats. The in-vivo pharmacokinetics study also proved a controlled delivery of cisplatin with enhanced mean residual time and half-life. Our studies suggested that the cisplatin-loaded LPHNP being a promising platform for controlled delivery of cisplatin in cancer therapy.

Keywords: cisplatin, lipid-polymer hybrid nanoparticle, chitosan, in vitro cell line study

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1872 The Chemical Transport Mechanism of Emitter Micro-Particles in Tungsten Electrode: A Metallurgical Study

Authors: G. Singh, H.Schuster, U. Füssel

Abstract:

The stability of electric arc and durability of electrode tip used in Tungsten Inert Gas (TIG) welding demand a metallurgical study about the chemical transport mechanism of emitter oxide particles in tungsten electrode during its real welding conditions. The tungsten electrodes doped with emitter oxides of rare earth oxides such as La₂O₃, Th₂O₃, Y₂O₃, CeO₂ and ZrO₂ feature a comparatively lower work function than tungsten and thus have superior emission characteristics due to lesser surface temperature of the cathode. The local change in concentration of these emitter particles in tungsten electrode due to high temperature diffusion (chemical transport) can change its functional properties like electrode temperature, work function, electron emission, and stability of the electrode tip shape. The resulting increment in tip surface temperature results in the electrode material loss. It was also observed that the tungsten recrystallizes to large grains at high temperature. When the shape of grain boundaries are granular in shape, the intergranular diffusion of oxide emitter particles takes more time to reach the electrode surface. In the experimental work, the microstructure of the used electrode's tip surface will be studied by scanning electron microscope and reflective X-ray technique in order to gauge the extent of the diffusion and chemical reaction of emitter particles. Besides, a simulated model is proposed to explain the effect of oxide particles diffusion on the electrode’s microstructure, electron emission characteristics, and electrode tip erosion. This model suggests metallurgical modifications in tungsten electrode to enhance its erosion resistance.

Keywords: rare-earth emitter particles, temperature-dependent diffusion, TIG welding, Tungsten electrode

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1871 Utilization of Sphagnum Moss as a Jeepney Emission Filter for Smoke Density Reduction

Authors: Monique Joyce L. Disamburum, Nicole C. Faustino, Ashley Angela A. Fazon, Jessie F. Rubonal

Abstract:

Traditional jeepneys contribute significantly to air pollution in the Philippines, negatively affecting both the environment and people. In response, the researchers investigated Sphagnum moss which has high adsorbent properties and can be used as a filter. Therefore, this research aims to create a muffler filter additive to reduce the smoke density emitted by traditional jeepneys. Various materials, such as moss, cornstarch, a metal pipe, bolts, and a papermaking screen frame, were gathered. The moss underwent a blending process with a cornstarch mixture until it achieved a pulp-like consistency, subsequently molded using a papermaking screen frame and left for sun drying. Following this, a metal prototype was created by drilling holes around the tumbler and inserting bolts. The mesh wire containing the filter was carefully placed into the hole, secured by two bolts. In the final phase, there were three setups, each undergoing one trial in the LTO emission testing. Each trial consisted of six rounds of purging, and after that the average smoke density was measured. According to the findings of this study, the filter aided in lowering the average smoke density. The one layer setup produced an average of 1.521, whereas the two layer setup produced an average of 1.082. Using One-Way Anova, it was demonstrated that there is a significant difference between the setups. Furthermore, the Tukey HSD Post Hoc test revealed that Setups A and C differed significantly (p = 0.04604), with Setup C being the most successful in reducing smoke density (mean difference -1.4128). Overall, the researchers came to the conclusion that employing Sphagnum moss as a filter can lower the average smoke density released by traditional jeepneys.

Keywords: sphagnum moss, Jeepney filter, smoke density, Jeepney emission

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1870 Current Methods for Drug Property Prediction in the Real World

Authors: Jacob Green, Cecilia Cabrera, Maximilian Jakobs, Andrea Dimitracopoulos, Mark van der Wilk, Ryan Greenhalgh

Abstract:

Predicting drug properties is key in drug discovery to enable de-risking of assets before expensive clinical trials and to find highly active compounds faster. Interest from the machine learning community has led to the release of a variety of benchmark datasets and proposed methods. However, it remains unclear for practitioners which method or approach is most suitable, as different papers benchmark on different datasets and methods, leading to varying conclusions that are not easily compared. Our large-scale empirical study links together numerous earlier works on different datasets and methods, thus offering a comprehensive overview of the existing property classes, datasets, and their interactions with different methods. We emphasise the importance of uncertainty quantification and the time and, therefore, cost of applying these methods in the drug development decision-making cycle. To the best of the author's knowledge, it has been observed that the optimal approach varies depending on the dataset and that engineered features with classical machine learning methods often outperform deep learning. Specifically, QSAR datasets are typically best analysed with classical methods such as Gaussian Processes, while ADMET datasets are sometimes better described by Trees or deep learning methods such as Graph Neural Networks or language models. Our work highlights that practitioners do not yet have a straightforward, black-box procedure to rely on and sets a precedent for creating practitioner-relevant benchmarks. Deep learning approaches must be proven on these benchmarks to become the practical method of choice in drug property prediction.

Keywords: activity (QSAR), ADMET, classical methods, drug property prediction, empirical study, machine learning

Procedia PDF Downloads 83
1869 Digitizing Masterpieces in Italian Museums: Techniques, Challenges and Consequences from Giotto to Caravaggio

Authors: Ginevra Addis

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The possibility of reproducing physical artifacts in a digital format is one of the opportunities offered by the technological advancements in information and communication most frequently promoted by museums. Indeed, the study and conservation of our cultural heritage have seen significant advancement due to the three-dimensional acquisition and modeling technology. A variety of laser scanning systems has been developed, based either on optical triangulation or on time-of-flight measurement, capable of producing digital 3D images of complex structures with high resolution and accuracy. It is necessary, however, to explore the challenges and opportunities that this practice brings within museums. The purpose of this paper is to understand what change is introduced by digital techniques in those museums that are hosting digital masterpieces. The methodology used will investigate three distinguished Italian exhibitions, related to the territory of Milan, trying to analyze the following issues about museum practices: 1) how digitizing art masterpieces increases the number of visitors; 2) what the need that calls for the digitization of artworks; 3) which techniques are most used; 4) what the setting is; 5) the consequences of a non-publication of hard copies of catalogues; 6) envision of these practices in the future. Findings will show how interconnection plays an important role in rebuilding a collection spread all over the world. Secondly how digital artwork duplication and extension of reality entail new forms of accessibility. Thirdly, that collection and preservation through digitization of images have both a social and educational mission. Fourthly, that convergence of the properties of different media (such as web, radio) is key to encourage people to get actively involved in digital exhibitions. The present analysis will suggest further research that should create museum models and interaction spaces that act as catalysts for innovation.

Keywords: digital masterpieces, education, interconnection, Italian museums, preservation

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1868 Biofuel Production via Thermal Cracking of Castor Methyl Ester

Authors: Roghaieh Parvizsedghy, Seyed Mojtaba Sadrameli

Abstract:

Diminishing oil reserves, deteriorating health standards because of greenhouse gas emissions and associated environmental impacts have emerged biofuel production. Vegetable oils are proved to be valuable feedstock in these growing industries as they are renewable and potentially inexhaustible sources. Thermal Cracking of vegetable oils (triglycerides) leads to production of biofuels which are similar to fossil fuels in terms of composition but their combustion and physical properties have limits. Acrolein (very poisonous gas) and water production during cracking of triglycerides occurs because of presence of glycerin in their molecular structure. Transesterification of vegetable oil is a method to extract glycerol from triglycerides structure and produce methyl ester. In this study, castor methyl ester was used for thermal cracking in order to survey the efficiency of this method to produce bio-gasoline and bio-diesel. Thus, several experiments were designed by means of central composite method. Statistical studies showed that two reaction parameters, namely cracking temperature and feed flowrate, affect products yield significantly. At the optimized conditions (480 °C and 29 g/h) for maximum bio-gasoline production, 88.6% bio-oil was achieved which was distilled and separated as bio-gasoline (28%) and bio-diesel (48.2%). Bio-gasoline exposed a high octane number and combustion heat. Distillation curve and Reid vapor pressure of bio-gasoline fell in the criteria of standard gasoline (class AA) by ASTM D4814. Bio-diesel was compatible with standard diesel by ASTM D975. Water production was negligible and no evidence of acrolein production was distinguished. Therefore, thermal cracking of castor methyl ester could be used as a method to produce valuable biofuels.

Keywords: bio-diesel, bio-gasoline, castor methyl ester, thermal cracking, transesterification

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1867 Effects of Application of Rice Husk Charcoal-Coated Urea and Rice Straw Compost on Growth, Yield, and Properties of Lowland Rice

Authors: D. A. S. Gamage, B. F. A. Basnayake, W.A.J.M. De Costa

Abstract:

Rice is the staple food of Sri Lankans thus; rice cultivation is the major agricultural activity of the country. The application of inorganic fertilizer has become a burden to the country. The excessive application of organic and inorganic fertilizers can potentially lead to deterioration of the quality of water. In mixing both urea and rice husk charcoal and rice straw compost in soils causes a slow release of nitrogen fertilizer, thus reducing the cost of importations of nitrogen based fertilizers per unit area of cultivation. Objective of this study was to evaluate rice husk charcoal coated urea as a slow releasing fertilizer and compare the total N,P, K, organic matter in soil and yield of rice production. Five treatments were used for twenty pots (pot size 30 cm diameter and 45 cm height) each replicated four times as: inorganic fertilizer only (Urea, TSP and MOP) (Treatment 1); rice husk charcoal coated urea, TSP and MOP (Treatment 2); inorganic fertilizer (Urea, TSP and MOP) with rice straw compost only (Treatment 3); rice husk charcoal urea, TSP and MOP with rice straw compost (Treatment 4); and no fertilizer as the control (Treatment 5). Rice grain yield was significantly higher in treatment 4 where rice husk charcoal coated urea, TSP and MOP with rice straw compost. The lowest yield was observed in control (treatment 5). The lower the value of the nitrogen to phosphorous ratio in soil, it indicates higher uptake of phosphorous. Charcoal can be used as a soil amendment and organic fertilizer, but adjustment of pH was required at high application rates. K content of soil of treatment 3 and 4 were the highest with compared to the treatment 1. Rice husk charcoal coated urea can potentially be used as a slow releasing nitrogen fertilizer.

Keywords: charcoal, rice husk, nitrogen to phosphorous ratio, soil amendment

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1866 Quartz Crystal Microbalance Based Hydrophobic Nanosensor for Lysozyme Detection

Authors: F. Yılmaz, Y. Saylan, A. Derazshamshir, S. Atay, A. Denizli

Abstract:

Quartz crystal microbalance (QCM), high-resolution mass-sensing technique, measures changes in mass on oscillating quartz crystal surface by measuring changes in oscillation frequency of crystal in real time. Protein adsorption techniques via hydrophobic interaction between protein and solid support, called hydrophobic interaction chromatography (HIC), can be favorable in many cases. Some nanoparticles can be effectively applied for HIC. HIC takes advantage of the hydrophobicity of proteins by promoting its separation on the basis of hydrophobic interactions between immobilized hydrophobic ligands and nonpolar regions on the surface of the proteins. Lysozyme is found in a variety of vertebrate cells and secretions, such as spleen, milk, tears, and egg white. Its common applications are as a cell-disrupting agent for extraction of bacterial intracellular products, as an antibacterial agent in ophthalmologic preparations, as a food additive in milk products and as a drug for treatment of ulcers and infections. Lysozyme has also been used in cancer chemotherapy. The aim of this study is the synthesis of hydrophobic nanoparticles for Lysozyme detection. For this purpose, methacryoyl-L-phenylalanine was chosen as a hydrophobic matrix. The hydrophobic nanoparticles were synthesized by micro-emulsion polymerization method. Then, hydrophobic QCM nanosensor was characterized by Attenuated total reflection Fourier transform infrared (ATR-FTIR) spectroscopy, atomic force microscopy (AFM) and zeta size analysis. Hydrophobic QCM nanosensor was tested for real-time detection of Lysozyme from aqueous solution. The kinetic and affinity studies were determined by using Lysozyme solutions with different concentrations. The responses related to a mass (Δm) and frequency (Δf) shifts were used to evaluate adsorption properties.

Keywords: nanosensor, HIC, lysozyme, QCM

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1865 Therapeutic Effect of Diisopropyldithiocarbamate Sodium Salt Against Diclofenac Induced Testicular Damage in Male Wistar Rats

Authors: Tella Toluwani, Adegbegi Ademuyiwa, Musei Chiedu, Adekunle Odola, Ayangbenro Ayansina, Adaramoye Oluwatosin

Abstract:

Dithiocarbamates are very useful biological agents with antioxidant properties. Diclofenac (DIC) is a non-steroidal analgesic, anti-inflammatory, and antipyretic agent. The use of diclofenac has been linked with reproductive toxicity/damage. The purpose of this study is (i) To investigate the therapeutic potential of diisopropyldithiocarbamate sodium salt (Na(i-Pr₂dtc)) and vitamin E (VIT E) against diclofenac induced toxicity in the testes of male Wistar rats. (ii) To investigate the effect of (Na(i-Pr₂dtc)) and vitamin E on ameliorating damage done to the testes through histological analysis of the testes. Thirty-six (36) male Wistar rats were used for the experiment, they were divided into six (6) groups, the animals in group 1 served as control, animals in groups 2, 3, 4, 5 and 6 received DIC only, DIC and (Na(i-Pr₂dtc)), DIC and VIT E, (Na(i-Pr₂dtc) only and VIT E only respectively. A single dose of 100 mg/kg body weight of DIC was administered to male Wistar rats, while 30 mg/kg body weight of (Na(i-Pr₂dtc)) was used to treat both normal and DIC treated animals, control animals were treated with the vehicle, after 24 hrs of treatment the animals were euthanized and the testes were removed for analysis. The treatment of rats with Na(i-Pr₂dtc) significantly restored catalase (CAT) activity depressed by diclofenac. (Na(i-Pr₂dtc)) also restored glutathione levels reduced by DIC treatment and this was also accompanied by reduced lipid peroxidation (LPO) level. VIT E significantly restored superoxide dismutase (SOD) activity when compared with DIC only treated animals. Photomicrographs of testes from (Na(i-Pr₂dtc)) treated rats showed seminiferous epithelium with no lesions. We conclude that (Na(i-Pr₂dtc)) has an antioxidant effect, which might be related to the dose and duration of administration.

Keywords: diisopropyldithiocarbamate sodium salt, diclofenac, vitamin E, testes

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1864 Microvoid Growth in the Interfaces during Aging

Authors: Jae-Yong Park, Gwancheol Seo, Young-Ho Kim

Abstract:

Microvoids, sometimes called Kikendall voids, generally form in the interfaces between Sn-based solders and Cu and degrade the mechanical and electrical properties of the solder joints. The microvoid formation is known as the rapid interdiffusion between Sn and Cu and impurity content in the Cu. Cu electroplating from the acid solutions has been widely used by microelectronic packaging industry for both printed circuit board (PCB) and integrated circuit (IC) applications. The quality of electroplated Cu that can be optimized by the electroplating conditions is critical for the solder joint reliability. In this paper, the influence of electroplating conditions on the microvoid growth in the interfaces between Sn-3.0Ag-0.5Cu (SAC) solder and Cu layer was investigated during isothermal aging. The Cu layers were electroplated by controlling the additive of electroplating bath and current density to induce various microvoid densities. The electroplating bath consisted of sulfate, sulfuric acid, and additives and the current density of 5-15 mA/cm2 for each bath was used. After aging at 180 °C for up to 250 h, typical bi-layer of Cu6Sn5 and Cu3Sn intermetallic compounds (IMCs) was gradually growth at the SAC/Cu interface and microvoid density in the Cu3Sn showed disparities in the electroplating conditions. As the current density increased, the microvoid formation was accelerated in all electroplating baths. The higher current density induced, the higher impurity content in the electroplated Cu. When the polyethylene glycol (PEG) and Cl- ion were mixed in an electroplating bath, the microvoid formation was the highest compared to other electroplating baths. On the other hand, the overall IMC thickness was similar in all samples irrespective of the electroplating conditions. Impurity content in electroplated Cu influenced the microvoid growth, but the IMC growth was not affected by the impurity content. In conclusion, the electroplated conditions are properly optimized to avoid the excessive microvoid formation that results in brittle fracture of solder joint under high strain rate loading.

Keywords: electroplating, additive, microvoid, intermetallic compound

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1863 Drape Simulation by Commercial Software and Subjective Assessment of Virtual Drape

Authors: Evrim Buyukaslan, Simona Jevsnik, Fatma Kalaoglu

Abstract:

Simulation of fabrics is more difficult than any other simulation due to complex mechanics of fabrics. Most of the virtual garment simulation software use mass-spring model and incorporate fabric mechanics into simulation models. The accuracy and fidelity of these virtual garment simulation software is a question mark. Drape is a subjective phenomenon and evaluation of drape has been studied since 1950’s. On the other hand, fabric and garment simulation is relatively new. Understanding drape perception of subjects when looking at fabric simulations is critical as virtual try-on becomes more of an issue by enhanced online apparel sales. Projected future of online apparel retailing is that users may view their avatars and try-on the garment on their avatars in the virtual environment. It is a well-known fact that users will not be eager to accept this innovative technology unless it is realistic enough. Therefore, it is essential to understand what users see when they are displaying fabrics in a virtual environment. Are they able to distinguish the differences between various fabrics in virtual environment? The purpose of this study is to investigate human perception when looking at a virtual fabric and determine the most visually noticeable drape parameter. To this end, five different fabrics are mechanically tested, and their drape simulations are generated by commercial garment simulation software (Optitex®). The simulation images are processed by an image analysis software to calculate drape parameters namely; drape coefficient, node severity, and peak angles. A questionnaire is developed to evaluate drape properties subjectively in a virtual environment. Drape simulation images are shown to 27 subjects and asked to rank the samples according to their questioned drape property. The answers are compared to the calculated drape parameters. The results show that subjects are quite sensitive to drape coefficient changes while they are not very sensitive to changes in node dimensions and node distributions.

Keywords: drape simulation, drape evaluation, fabric mechanics, virtual fabric

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1862 Influence of Infinite Elements in Vibration Analysis of High-Speed Railway Track

Authors: Janaki Rama Raju Patchamatla, Emani Pavan Kumar

Abstract:

The idea of increasing the existing train speeds and introduction of the high-speed trains in India as a part of Vision-2020 is really challenging from both economic viability and technical feasibility. More than economic viability, technical feasibility has to be thoroughly checked for safe operation and execution. Trains moving at high speeds need a well-established firm and safe track thoroughly tested against vibration effects. With increased speeds of trains, the track structure and layered soil-structure interaction have to be critically assessed for vibration and displacements. Physical establishment of track, testing and experimentation is a costly and time taking process. Software-based modelling and simulation give relatively reliable, cost-effective means of testing effects of critical parameters like sleeper design and density, properties of track and sub-grade, etc. The present paper reports the applicability of infinite elements in reducing the unrealistic stress-wave reflections from so-called soil-structure interface. The influence of the infinite elements is quantified in terms of the displacement time histories of adjoining soil and the deformation pattern in general. In addition, the railhead response histories at various locations show that the numerical model is realistic without any aberrations at the boundaries. The numerical model is quite promising in its ability to simulate the critical parameters of track design.

Keywords: high speed railway track, finite element method, Infinite elements, vibration analysis, soil-structure interface

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1861 Numerical Investigation of the Needle Opening Process in a High Pressure Gas Injector

Authors: Matthias Banholzer, Hagen Müller, Michael Pfitzner

Abstract:

Gas internal combustion engines are widely used as propulsion systems or in power plants to generate heat and electricity. While there are different types of injection methods including the manifold port fuel injection and the direct injection, the latter has more potential to increase the specific power by avoiding air displacement in the intake and to reduce combustion anomalies such as backfire or pre-ignition. During the opening process of the injector, multiple flow regimes occur: subsonic, transonic and supersonic. To cover the wide range of Mach numbers a compressible pressure-based solver is used. While the standard Pressure Implicit with Splitting of Operators (PISO) method is used for the coupling between velocity and pressure, a high-resolution non-oscillatory central scheme established by Kurganov and Tadmor calculates the convective fluxes. A blending function based on the local Mach- and CFL-number switches between the compressible and incompressible regimes of the developed model. As the considered operating points are well above the critical state of the used fluids, the ideal gas assumption is not valid anymore. For the real gas thermodynamics, the models based on the Soave-Redlich-Kwong equation of state were implemented. The caloric properties are corrected using a departure formalism, for the viscosity and the thermal conductivity the empirical correlation of Chung is used. For the injector geometry, the dimensions of a diesel injector were adapted. Simulations were performed using different nozzle and needle geometries and opening curves. It can be clearly seen that there is a significant influence of all three parameters.

Keywords: high pressure gas injection, hybrid solver, hydrogen injection, needle opening process, real-gas thermodynamics

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1860 Use of Geosynthetics as Reinforcement Elements in Unpaved Tertiary Roads

Authors: Vivian A. Galindo, Maria C. Galvis, Jaime R. Obando, Alvaro Guarin

Abstract:

In Colombia, most of the roads of the national tertiary road network are unpaved roads with granular rolling surface. These are very important ways of guaranteeing the mobility of people, products, and inputs from the agricultural sector from the most remote areas to urban centers; however, it has not paid much attention to the search for alternatives to avoid the occurrence of deteriorations that occur shortly after its commissioning. In recent years, geosynthetics have been used satisfactorily to reinforce unpaved roads on soft soils, with geotextiles and geogrids being the most widely used. The interaction of the geogrid and the aggregate minimizes the lateral movement of the aggregate particles and increases the load capacity of the material, which leads to a better distribution of the vertical stresses, consequently reducing the vertical deformations in the subgrade. Taking into account the above, the research aimed at the mechanical behavior of the granular material, used in unpaved roads with and without the presence of geogrids, from the development of laboratory tests through the loaded wheel tester (LWT). For comparison purposes, the reinforced conditions and traffic conditions to which this type of material can be accessed in practice were simulated. In total four types of geogrids, were tested with granular material; this means that five test sets, the reinforced material and the non-reinforced control sample were evaluated. The results of the numbers of load cycles and depth rutting supported by each test body showed the influence of the properties of the reinforcement on the mechanical behavior of the assembly and the significant increases in the number of load cycles of the reinforced specimens in relation to those without reinforcement.

Keywords: geosynthetics, load wheel tester LWT, tertiary roads, unpaved road, vertical deformation

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1859 Development of Patient Satisfaction Questionnaire for Diabetes Management in Thailand and Lao People Democratic Republic

Authors: Phoutsathaphone Sibounheuang, Phayom Sookaneknun Olson, Chanuttha Ploylearmsang, Santiparp Sookaneknun, Chanthanom Manithip

Abstract:

Patient satisfaction is an outcome that can be measured and used to improve diabetes care and management. There are limited instruments for assessing patient satisfaction covering the whole process of diabetes management. In this study, the questionnaire was developed with items pooled from a systematic review of qualitative studies of patients’ and healthcare providers’ perspectives in diabetes management. The questionnaire consists of 11 domains with 45 items. The Thai version was translated to Lao and then checked by back-translating it into Thai. We tested the questionnaire on 150 diabetes patients in Thailand and 150 in Lao People Democratic Republic (PDR). Validity was performed by factor analysis and Pearson correlation. Internal consistency reliability was estimated by calculating Cronbach’s alpha. The study was approved by the Mahasarakham University Ethics Committee, and the National Ethics Committee for Health Research, Lao PDR. The Thai and Lao versions showed the construct validity by principal component analysis. This consisted of 11 domains which account for 71.23% of the variance (Thai version) and 71.66% of the variance (Lao version) in the total patient satisfaction scores. The Kaiser-Meyer-Olkin (KMO) measures were 0.85 for the Thai version and 0.75 for the Lao version. The Bartlett tests of sphericity of both versions were significant (p < 0.001). The factor loadings of all items in both versions were > 0.40. The convergent validity of the Thai and Lao versions was 93.63% and 79.54% respectively. The discriminant validity for the Thai and Lao versions was 92.68% and 88.68% respectively. Cronbach’s alpha was 0.95 in both versions. The Patient Satisfaction Questionnaire (PSQ) in both versions had acceptable properties. This study has yielded evidence supporting the validity and reliability of both versions.

Keywords: construct validity, diabetes management, patient satisfaction, questionnaire development, reliability

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1858 Effects of Drought on Microbial Activity in Rhizosphere, Soil Hydrophobicity and Leaching of Mineral Nitrogen from Arable Soil Depending on Method of Fertilization

Authors: Jakub Elbl, Lukáš Plošek, Antonín Kintl, Jaroslav Hynšt, Soňa Javoreková, Jaroslav Záhora, Libor Kalhotka, Olga Urbánková, Ivana Charousová

Abstract:

This work presents the first results from the long-term laboratory experiment dealing with impact of drought on soil properties. Three groups of the treatment (A, B and C) with different regime of irrigation were prepared. The soil water content was maintained at 70 % of soil water holding capacity in group A, at 40 % in group B. In group C, soil water regime was maintained in the range of wilting point. Each group of the experiment was divided into three variants (A1 = B1, C1; A2 = B2, C2 etc.) with three repetitions: Variants A1 (B1, C1) were controls without addition of another fertilizer. Variants A2 (B2, C2) were fertilized with mineral nitrogen fertilizer DAM 390 (0.140 Mg of N per ha) and variants A3 (B3, C3) contained 45 g of Cp per a pot. The significant differences (ANOVA, P<0.05) in the leaching of mineral nitrogen and values of saturated hydraulic conductivity (Ksat) were found. The highest values of Ksat were found in variants (within each group) with addition of compost (A3, B3, C3). Conversely, the lowest values of Ksat were found in variants with addition of mineral nitrogen. Low values of Ksat indicate an increased level of hydrophobicity in individual groups of the experiment. Moreover, all variants with compost addition showed lower amount of mineral nitrogen leaching and high level of microbial activity than variants without. This decrease of mineral nitrogen leaching was about 200 % in comparison with the control variant and about 300 % with variant, where mineral nitrogen was added. Based on these results, we can conclude that changes of soil water content directly have impact on microbial activity, soil hydrophobicity and loss of mineral nitrogen from the soil.

Keywords: drought, microbial activity, mineral nitrogen, soil hydrophobicity

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1857 Design and Characterization of Ecological Materials Based on Demolition and Concrete Waste, Casablanca (Morocco)

Authors: Mourad Morsli, Mohamed Tahiri, Azzedine Samdi

Abstract:

The Cities are the urbanized territories most favorable to the consumption of resources (materials, energy). In Morocco, the economic capital Casablanca is one of them, with its 4M inhabitants and its 60% share in the economic and industrial activity of the kingdom. In the absence of legal status in force, urban development has favored the generation of millions of tons of demolition and construction waste scattered in open spaces causing a significant nuisance to the environment and citizens. Hence the main objective of our work is to valorize concrete waste. The representative wastes are mainly concrete, concrete, and fired clay bricks, ceramic tiles, marble panels, gypsum, and scrap metal. The work carried out includes: geolocation with a combination of artificial intelligence, GIS, and Google Earth, which allowed the estimation of the quantity of these wastes per site; then the sorting, crushing, grinding, and physicochemical characterization of the collected samples allowed the definition of the exploitation ways for each extracted fraction for integrated management of the said wastes. In the present work, we proceeded to the exploitation of the fractions obtained after sieving the representative samples to incorporate them in the manufacture of new ecological materials for construction. These formulations prepared studies have been tested and characterized: physical criteria (specific surface, resistance to flexion and compression) and appearance (cracks, deformation). We will present in detail the main results of our research work and also describe the specific properties of each material developed.

Keywords: demolition and construction waste, GIS combination software, inert waste recovery, ecological materials, Casablanca, Morocco

Procedia PDF Downloads 136
1856 An Overview of Pakistani Shales for Shale Gas Exploration and Comparison to North American Shale Plays

Authors: Ghulam Sohail, Christopher Hawkes

Abstract:

Pakistan has been facing a growing energy crisis for the last decade, and the government is seeking new horizons for increasing oil and gas production to reduce the gap between supply and demand. Recent developments in technologies to produce natural gas from shales at economical rates has unlocked new horizons for hydrocarbon exploration and development throughout the world. Operating companies in the U.S.A. and Canada have been particularly successful at producing shale gas, so comparing against the properties of shale gas reservoirs in these countries is used for an initial assessment of prospective shale gas reservoirs in other parts of the world. In this study, selected source rocks of Pakistan are evaluated for their shale gas potential using analogs selected from various North American shales for which data have been published. Published data for Pakistani shales were compiled, then assessed and supplemented through consultation with industry professionals. Pakistani formations reviewed are the Datta (shaly sandstone), Hangu (sandy shale), Patala (sandy shale), Ranikot (shaly sandstone), Sembar (sandy shale) and Lower Goru (shaly sandstone) formations, all of which are known source rocks in the Indus Basin. For this study, available geological, geochemical, petrophysical and elastic parameters have been investigated and are correlated specifically with the eight most active shale gas plays of the U.S.A., while data for other North American shale gas plays are used for general discussion on prospective Pakistani shales. The results show that the geological and geochemical parameters of all the Pakistani shales reviewed in this work are promising regarding their shale gas. However, more petrophysical and geomechanical data are required before conclusions on economic production from these shales can be made with confidence.

Keywords: Canada shale gas, Indus Basin, Pakistani shales, U.S.A shale gas

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1855 Mechanisms and Regulation of the Bi-directional Motility of Mitotic Kinesin Nano-motors

Authors: Larisa Gheber

Abstract:

Mitosis is an essential process by which duplicated genetic information is transmitted from mother to daughter cells. Incorrect chromosome segregation during mitosis can lead to genetic diseases, chromosome instability and cancer. This process is mediated by a dynamic microtubule-based intracellular structure, the mitotic spindle. One of the major factors that govern the mitotic spindle dynamics are the kinesin-5 biological nano motors that were believed to move unidirectionally on the microtubule filaments, using ATP hydrolysis, thus performing essential functions in mitotic spindle dynamics. Surprisingly, several reports from our and other laboratories have demonstrated that some kinesin-5 motors are bi-directional: they move in minus-end direction on the microtubules as single-molecules and can switch directionality under a number of conditions. These findings broke a twenty-five-years old dogma regarding kinesin directionality (1, 2). The mechanism of this bi-directional motility and its physiological significance remain unclear. To address this unresolved problem, we apply an interdisciplinary approach combining live cell imaging, biophysical single molecule, and structural experiments to examine the activity of these motors and their mutated variants in vivo and in vitro. Our data shows that factors such as protein phosphorylation (3, 4), motor clustering on the microtubules (5, 6) and structural elements (7, 8) regulate the bi-directional motility of kinesin motors. We also show, using Cryo-EM, that bi-directional kinesin motors obtain non-canonical microtubule binding, which is essential to their special motile properties and intracellular functions. We will discuss the implication of these findings to mechanism bi-directional motility and physiological roles in mitosis.

Keywords: mitosis, cancer, kinesin, microtubules, biochemistry, biophysics

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1854 Investigating the Role of Lactiplantibacillus Plantarum vs. Spontaneous Fermentation in Improving Nutritional and Consumer Safety of the Fermented White Cabbage Sprouts

Authors: Anam Layla, Qamar Abbas Syed, Tahir Zahoor, Muhammad Shahid

Abstract:

Brassicaceae sprouts are promising candidates for functional food because of their unique phytochemistry and high nutrient density compared to their seeds and matured vegetables. Despite being admired for their health-promoting properties, white cabbage sprouts have been least explored for their nutritional significance and behavior to lactic acid fermentation. This study aimed to investigate the role of lactic acid fermentation i.e., inoculum vs. spontaneous, in reducing intrinsic toxicants load and improving nutrients delivering potential of the white cabbage sprouts. White cabbage sprouts with a 5 – 7 cm average size were processed as raw, blanched, Lactiplantibacillus plantarum inoculated fermentation and spontaneous fermentation. Plant material was dehydrated at 40˚C and evaluated for microbiological quality, macronutrients, minerals, and anti-nutrient contents. The results indicate L. plantarum inoculum fermentation of blanched cabbage sprouts (IF-BCS) to increase lactic acid bacteria count of the sprouts from 0.97 to 8.47 log CFU/g. Compared with the raw cabbage sprouts (RCS), inoculum fermented-raw cabbage sprouts (IF-RCS), and spontaneous fermented-raw cabbage sprouts (SF-RCS), the highest content of Ca (447 mg/ 100g d.w.), Mg (204 mg/100g d.w.), Fe (9.3 mg/100g d.w.), Zn (5 mg/100g d.w.) and Cu (0.5 mg/100g d.w.) were recorded in IF-BCS. L. plantarum led fermentation of BCS demonstrated a reduction in phytates, tannins, and oxalates contents at a rate of 42%, 66%, and 53%, respectively, while standalone lactic acid fermentation of the raw sprouts reduced the burden of anti-nutrients in a range between 32 to 56%. The results suggest L. plantarum led lactic acid fermentation coupled with sprouts blanching is the most promising way to improve the nutritional quality and safety of the white cabbage sprouts.

Keywords: lactic acid fermentation, anti-nutrients, mineral content, nutritional quality

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1853 Design of the Compliant Mechanism of a Biomechanical Assistive Device for the Knee

Authors: Kevin Giraldo, Juan A. Gallego, Uriel Zapata, Fanny L. Casado

Abstract:

Compliant mechanisms are designed to deform in a controlled manner in response to external forces, utilizing the flexibility of their components to store potential elastic energy during deformation, gradually releasing it upon returning to its original form. This article explores the design of a knee orthosis intended to assist users during stand-up motion. The orthosis makes use of a compliant mechanism to balance the user’s weight, thereby minimizing the strain on leg muscles during standup motion. The primary function of the compliant mechanism is to store and exchange potential energy, so when coupled with the gravitational potential of the user, the total potential energy variation is minimized. The design process for the semi-rigid knee orthosis involved material selection and the development of a numerical model for the compliant mechanism seen as a spring. Geometric properties are obtained through the numerical modeling of the spring once the desired stiffness and safety factor values have been attained. Subsequently, a 3D finite element analysis was conducted. The study demonstrates a strong correlation between the maximum stress in the mathematical model (250.22 MPa) and the simulation (239.8 MPa), with a 4.16% error. Both analyses safety factors: 1.02 for the mathematical approach and 1.1 for the simulation, with a consistent 7.84% margin of error. The spring’s stiffness, calculated at 90.82 Nm/rad analytically and 85.71 Nm/rad in the simulation, exhibits a 5.62% difference. These results suggest significant potential for the proposed device in assisting patients with knee orthopedic restrictions, contributing to ongoing efforts in advancing the understanding and treatment of knee osteoarthritis.

Keywords: biomechanics, complaint mechanisms, gonarthrosis, orthoses

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1852 Human Metabolism of the Drug Candidate PBTZ169

Authors: Vadim Makarov, Stewart T.Cole

Abstract:

PBTZ169 is novel drug candidate with high efficacy in animals models, and its combination treatment of PBTZ169 with BDQ and pyrazinamide was shown to be more efficacious than the standard treatment for tuberculosis in a mouse model. The target of PBTZ169 is famous DprE1, an essential enzyme in cell wall biosynthesis. The crystal structure of the DprE1-PBTZ169 complex reveals formation of a semimercaptal adduct with Cys387 in the active site and explains the irreversible inactivation of the enzyme. Furthermore, this drug candidate demonstrated during preclinical research ‘drug like’ properties what made it an attractive drug candidate to treat tuberculosis in humans. During first clinical trials several cohorts of the healthy volunteers were treated by the single doses of PBTZ169 as well as two weeks repeated treatment was chosen for two maximal doses. As expected PBTZ169 was well tolerated, and no significant toxicity effects were observed during the trials. The study of the metabolism shown that human metabolism of PBTZ169 is very different from microbial or animals compound transformation. So main pathway of microbial, mice and less rats metabolism connected with reduction processes, but human metabolism mainly connected with oxidation processes. Due to this difference we observed several metabolites of PBTZ169 in humans with antitubercular activity, and now we can conclude that animal antituberculosis activity of PBTZ169 is a result not only activity of the drug itself, but it is a result of the sum activity of the drug and its metabolites. Direct antimicrobial plasma activity was studied, and such activity was observed for 24 hours after human treatment for some doses. This data gets high chance for good efficacy of PBTZ169 in human for treatment TB infection. Second phase of clinical trials was started summer of 2017 and continues to the present day. Available data will be presented.

Keywords: clinical trials, DprE1, PBTZ169, metabolism

Procedia PDF Downloads 167