Search results for: docking operation
Commenced in January 2007
Frequency: Monthly
Edition: International
Paper Count: 2984

Search results for: docking operation

2414 Performance Assessment of a Variable-Flux Permanent-Magnet Memory Motor

Authors: Michel Han, Christophe Besson, Alain Savary, Yvan Becher

Abstract:

The variable flux permanent magnet synchronous motor (VF-PMSM), also called "Memory Motor", is a new generation of motor capable of modifying the magnetization state with short pulses of current during operation or standstill. The impact of such operation is the expansion of the operating range in the torque-speed characteristic and an improvement in energy efficiency at high-speed in comparison to conventional permanent magnet synchronous machines (PMSMs). This paper reviews the operating principle and the unique features of the proposed memory motor. The benefits of this concept are highlighted by comparing the performance of the rotor of the VF-PMSM to that of two PM rotors that are typically found in the industry. The investigation emphasizes the properties of the variable magnetization and presents the comparison of the torque-speed characteristic with the capability of loss reduction in a VF-PMSM by means of experimental results, especially when tests are conducted under identical conditions for each rotor (same stator, same inverter and same experimental setup). The experimental results demonstrated that the VF-PMSM gives an additional degree of freedom to optimize the efficiency over a wide speed range. Thus, with a design easy to manufacture and with the possibility of controlling the magnetization and the demagnetization of the magnets during operations, the VF-PMSM can be interesting for various applications.

Keywords: efficiency, magnetization state, memory motors, performances, permanent-magnet, synchronous machine, variable-flux, variable magnetization, wide speed application

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2413 A Molecular Modelling Approach for Identification of Lead Compound from Rhizomes of Glycosmis Pentaphylla for Skin Cancer Treatment

Authors: Rahul Shrivastava, Manish Tripathi, Mohmmad Yasir, Shailesh Singh

Abstract:

Life style changes and depletion in atmospheric ozone layer in recent decades lead to increase in skin cancer including both melanoma and nonmelanomas. Natural products which were obtained from different plant species have the potential of anti skin cancer activity. In regard of this, present study focuses the potential effect of Glycosmis pentaphylla against anti skin cancer activity. Different Phytochemical constituents which were present in the roots of Glycosmis pentaphylla were identified and were used as ligands after sketching of their structures with the help of ACD/Chemsketch. These ligands are screened for their anticancer potential with proteins which are involved in skin cancer effects with the help of pyrx software. After performing docking studies, results reveal that Noracronycine secondary metabolite of Glycosmis pentaphylla shows strong affinity of their binding energy with Ribosomal S6 Kinase 2 (2QR8) protein. Ribosomal S6 Kinase 2 (2QR8) has an important role in the cell proliferation and transformation mediated through by N-terminal kinase domain and was induced by the tumour promoters such as epidermal growth factor. It also plays a key role in the neoplastic transformation of human skin cells and in skin cancer growth. Noracronycine interact with THR-493 and MET-496 residue of Ribosomal S6 Kinase 2 protein with binding energy ΔG = -8.68 kcal/mole. Thus on the basis of this study we can say that Noracronycine which present in roots of Glycosmis pentaphylla can be used as lead compound against skin cancer.

Keywords: glycosmis pentaphylla, pyrx, ribosomal s6 kinase, skin cancer

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2412 Study on Heat Transfer Capacity Limits of Heat Pipe with Working Fluids Ammonia and Water

Authors: M. Heydari, A. Ghanami

Abstract:

Heat pipe is simple heat transfer device which combines the conduction and phase change phenomena to control the heat transfer without any need for external power source. At hot surface of heat pipe, the liquid phase absorbs heat and changes to vapor phase. The vapor phase flows to condenser region and with the loss of heat changes to liquid phase. Due to gravitational force the liquid phase flows to evaporator section. In HVAC systems the working fluid is chosen based on the operating temperature. The heat pipe has significant capability to reduce the humidity in HVAC systems. Each HVAC system which uses heater, humidifier or dryer is a suitable nominate for the utilization of heat pipes. Generally heat pipes have three main sections: condenser, adiabatic region, and evaporator. Performance investigation and optimization of heat pipes operation in order to increase their efficiency is crucial. In the present article, a parametric study is performed to improve the heat pipe performance. Therefore, the heat capacity of heat pipe with respect to geometrical and confining parameters is investigated. For the better observation of heat pipe operation in HVAC systems, a CFD simulation in Eulerian- Eulerian multiphase approach is also performed. The results show that heat pipe heat transfer capacity is higher for water as working fluid with the operating temperature of 340 K. It is also showed that the vertical orientation of heat pipe enhances it’s heat transfer capacity.used in the abstract.

Keywords: heat pipe, HVAC system, grooved heat pipe, heat pipe limits

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2411 Processes and Application of Casting Simulation and Its Software’s

Authors: Surinder Pal, Ajay Gupta, Johny Khajuria

Abstract:

Casting simulation helps visualize mold filling and casting solidification; predict related defects like cold shut, shrinkage porosity and hard spots; and optimize the casting design to achieve the desired quality with high yield. Flow and solidification of molten metals are, however, a very complex phenomenon that is difficult to simulate correctly by conventional computational techniques, especially when the part geometry is intricate and the required inputs (like thermo-physical properties and heat transfer coefficients) are not available. Simulation software is based on the process of modeling a real phenomenon with a set of mathematical formulas. It is, essentially, a program that allows the user to observe an operation through simulation without actually performing that operation. Simulation software is used widely to design equipment so that the final product will be as close to design specs as possible without expensive in process modification. Simulation software with real-time response is often used in gaming, but it also has important industrial applications. When the penalty for improper operation is costly, such as airplane pilots, nuclear power plant operators, or chemical plant operators, a mockup of the actual control panel is connected to a real-time simulation of the physical response, giving valuable training experience without fear of a disastrous outcome. The all casting simulation software has own requirements, like magma cast has only best for crack simulation. The latest generation software Auto CAST developed at IIT Bombay provides a host of functions to support method engineers, including part thickness visualization, core design, multi-cavity mold design with common gating and feeding, application of various feed aids (feeder sleeves, chills, padding, etc.), simulation of mold filling and casting solidification, automatic optimization of feeders and gating driven by the desired quality level, and what-if cost analysis. IIT Bombay has developed a set of applications for the foundry industry to improve casting yield and quality. Casting simulation is a fast and efficient solution for process for advanced tool which is the result of more than 20 years of collaboration with major industrial partners and academic institutions around the world. In this paper the process of casting simulation is studied.

Keywords: casting simulation software’s, simulation technique’s, casting simulation, processes

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2410 Synergistic Effect of Eugenol Acetate with Betalactam Antibiotic on Betalactamase and Its Bioinformatics Analysis

Authors: Vinod Nair, C. Sadasivan

Abstract:

Beta-lactam antibiotics are the most frequently prescribed medications in modern medicine. The antibiotic resistance by the production of enzyme beta-lactamase is an important mechanism seen in microorganisms. Resistance to beta-lactams mediated by beta-lactamases can be overcome successfully with the use of beta-lactamase inhibitors. New generations of the antibiotics contain mostly synthetic compounds, and many side effects have been reported for them. Combinations of beta-lactam and beta-lactamase inhibitors have become one of the most successful antimicrobial strategies in the current scenario of bacterial infections. Plant-based drugs are very cheap and having lesser adverse effect than synthetic compounds. The synergistic effect of eugenol acetate with beta-lactams restores the activity of beta-lactams, allowing their continued clinical use. It is reported here the enhanced inhibitory effect of phytochemical, eugenol acetate, isolated from the plant Syzygium aromaticum with beta-lactams on beta-lactamase. The compound was found to have synergistic effect with the antibiotic amoxicillin against antibiotic-resistant strain of S.aureus. The enzyme was purified from the organism and incubated with the compound. The assay showed that the compound could inhibit the enzymatic activity of beta-lactamase. Modeling and molecular docking studies indicated that the compound can fit into the active site of beta-lactamase and can mask the important residue for hydrolysis of beta-lactams. The synergistic effects of eugenol acetate with beta-lactam antibiotics may justify, the use of these plant compounds for the preparation of β-lactamase inhibitors against β-lactam resistant S.aureus.

Keywords: betalactamase, eugenol acetate, synergistic effect, molecular modeling

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2409 Using Building Information Modelling to Mitigate Risks Associated with Health and Safety in the Construction and Maintenance of Infrastructure Assets

Authors: Mohammed Muzafar, Darshan Ruikar

Abstract:

BIM, an acronym for Building Information Modelling relates to the practice of creating a computer generated model which is capable of displaying the planning, design, construction and operation of a structure. The resulting simulation is a data-rich, object-oriented, intelligent and parametric digital representation of the facility, from which views and data, appropriate to various users needs can be extracted and analysed to generate information that can be used to make decisions and to improve the process of delivering the facility. BIM also refers to a shift in culture that will influence the way the built environment and infrastructure operates and how it is delivered. One of the main issues of concern in the construction industry at present in the UK is its record on Health & Safety (H&S). It is, therefore, important that new technologies such as BIM are developed to help improve the quality of health and safety. Historically the H&S record of the construction industry in the UK is relatively poor as compared to the manufacturing industries. BIM and the digital environment it operates within now allow us to use design and construction data in a more intelligent way. It allows data generated by the design process to be re-purposed and contribute to improving efficiencies in other areas of a project. This evolutionary step in design is not only creating exciting opportunities for the designers themselves but it is also creating opportunity for every stakeholder in any given project. From designers, engineers, contractors through to H&S managers, BIM is accelerating a cultural change. The paper introduces the concept behind a research project that mitigates the H&S risks associated with the construction, operation and maintenance of assets through the adoption of BIM.

Keywords: building information modeling, BIM levels, health, safety, integration

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2408 In-silico Antimicrobial Activity of Bioactive Compounds of Ricinus communis against DNA Gyrase of Staphylococcus aureus as Molecular Target

Authors: S. Rajeswari

Abstract:

Medicinal Plant extracts and their bioactive compounds have been used for antimicrobial activities and have significant remedial properties. In the recent years, a wide range of investigations have been carried out throughout the world to confirm antimicrobial properties of different medicinally important plants. A number of plants showed efficient antimicrobial activities, which were comparable to that of synthetic standard drugs or antimicrobial agents. The large family Euphorbiaceae contains nearly about 300 genera and 7,500 speciesand one among is Ricinus communis or castor plant which has high traditional and medicinal value for disease free healthy life. Traditionally the plant is used as laxative, purgative, fertilizer and fungicide etc. whereas the plant possess beneficial effects such as anti-oxidant, antihistamine, antinociceptive, antiasthmatic, antiulcer, immunomodulatory anti diabetic, hepatoprotective, anti inflammatory, antimicrobial, and many other medicinal properties. This activity of the plant possess due to the important phytochemical constituents like flavonoids, saponins, glycosides, alkaloids and steroids. The presents study includes the phytochemical properties of Ricinus communis and to prediction of the anti-microbial activity of Ricinus communis using DNA gyrase of Staphylococcus aureus as molecular target. Docking results of varies chemicals compounds of Ricinus communis against DNA gyrase of Staphylococcus aureus by maestro 9.8 of Schrodinger show that the phytochemicals are effective against the target protein DNA gyrase. our studies suggest that the phytochemical from Ricinus communis such has INDICAN (G.Score 4.98) and SUPLOPIN-2(G.Score 5.74) can be used as lead molecule against Staphylococcus infections.

Keywords: euphorbiaceae, antimicrobial activity, Ricinus communis, Staphylococcus aureus

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2407 Selecting the Best Risk Exposure to Assess Collision Risks in Container Terminals

Authors: Mohammad Ali Hasanzadeh, Thierry Van Elslander, Eddy Van De Voorde

Abstract:

About 90 percent of world merchandise trade by volume being carried by sea. Maritime transport remains as back bone behind the international trade and globalization meanwhile all seaborne goods need using at least two ports as origin and destination. Amid seaborne traded cargos, container traffic is a prosperous market with about 16% in terms of volume. Albeit containerized cargos are less in terms of tonnage but, containers carry the highest value cargos amongst all. That is why efficient handling of containers in ports is very important. Accidents are the foremost causes that lead to port inefficiency and a surge in total transport cost. Having different port safety management systems (PSMS) in place, statistics on port accidents show that numerous accidents occur in ports. Some of them claim peoples’ life; others damage goods, vessels, port equipment and/or the environment. Several accident investigation illustrate that the most common accidents take place throughout transport operation, it sometimes accounts for 68.6% of all events, therefore providing a safer workplace depends on reducing collision risk. In order to quantify risks at the port area different variables can be used as exposure measurement. One of the main motives for defining and using exposure in studies related to infrastructure is to account for the differences in intensity of use, so as to make comparisons meaningful. In various researches related to handling containers in ports and intermodal terminals, different risk exposures and also the likelihood of each event have been selected. Vehicle collision within the port area (10-7 per kilometer of vehicle distance travelled) and dropping containers from cranes, forklift trucks, or rail mounted gantries (1 x 10-5 per lift) are some examples. According to the objective of the current research, three categories of accidents selected for collision risk assessment; fall of container during ship to shore operation, dropping container during transfer operation and collision between vehicles and objects within terminal area. Later on various consequences, exposure and probability identified for each accident. Hence, reducing collision risks profoundly rely on picking the right risk exposures and probability of selected accidents, to prevent collision accidents in container terminals and in the framework of risk calculations, such risk exposures and probabilities can be useful in assessing the effectiveness of safety programs in ports.

Keywords: container terminal, collision, seaborne trade, risk exposure, risk probability

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2406 Effect of Clerodendrum Species on Oxidative Stress with Possible Implication in Alleviating Carcinogenesis

Authors: Somit Dutta, Pallab Kar, Arnab Kumar Chakraborty, Arnab Sen, Tapas Kumar Chaudhuri

Abstract:

In the present study three species of Clerodendrum; Clerodendrum indicum, Volkameria inermis and Clerodendrum colebrookianum were used to investigate the possible activity against oxidative stress. A detailed in-vivo and in-vitro antioxidant profiling, directly associated with inflammation-related carcinogenesis, has been executed with a motive to evaluate the free radical scavenging activity of Clerodendrum extract. Measurement of cell viability and ROS generation in HEK-293 (Human Embryonic Kidney Cell Line) cells was also estimated. The immune cell proliferative properties (MTT) and in-vitro assay for evaluation of their antioxidant activities including hydroxyl radical, nitric oxide, singlet oxygen, peroxinitrate and hydrogen peroxide, etc. were investigated. GC-MS and FTIR analyses have been performed to identify the active biological compounds. These active biological compounds were further studied to assess their potential medicinal properties, aided by molecular docking and interaction analysis between the active compounds and different proteins related to oxidative stress leading to progression of carcinogenesis. The research article clearly demonstrates the role of ROS in various phases of carcinogenesis. Therefore, the antioxidant and free radical scavenging capacity of all the Clerodendrum species might prove beneficial for the immune system. It might be concluded that this plant species offers great promise for cancer prevention and therapy due to the presence of several bioactive compounds and potent antioxidant capacity of C. colebrookianum.

Keywords: antioxidant, cancer, oxidative stress, reactive oxygen species (ROS)

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2405 Revealing of the Wave-Like Process in Kinetics of the Structural Steel Radiation Degradation

Authors: E. A. Krasikov

Abstract:

Dependence of the materials properties on neutron irradiation intensity (flux) is a key problem while usage data of the accelerated materials irradiation in test reactors for forecasting of their capacity for work in realistic (practical) circumstances of operation. Investigations of the reactor pressure vessel steel radiation degradation dependence on fast neutron fluence (embrittlement kinetics) at low flux reveal the instability in the form of the scatter of the experimental data and wave-like sections of embrittlement kinetics appearance. Disclosure of the steel degradation oscillating is a sign of the steel structure cyclic self-recovery transformation as it take place in self-organization processes. This assumption has received support through the discovery of the similar ‘anomalous’ data in scientific publications and by means of own additional experiments. Data obtained stimulate looking-for ways to management of the structural steel radiation stability (for example, by means of nano - structure modification for radiation defects annihilation intensification) for creation of the intelligent self-recovering material. Expected results: - radiation degradation theory and mechanisms development, - more adequate models of the radiation embrittlement elaboration, - surveillance specimen programs improvement, - methods and facility development for usage data of the accelerated materials irradiation for forecasting of their capacity for work in realistic (practical) circumstances of operation, - search of the ways for creating of the radiation stable self-recovery intelligent materials.

Keywords: degradation, radiation, steel, wave-like kinetics

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2404 Energy Efficiency Improvement of Excavator with Independent Metering Valve by Continuous Mode Changing Considering Engine Fuel Consumption

Authors: Sang-Wook Lee, So-Yeon Jeon, Min-Gi Cho, Dae-Young Shin, Sung-Ho Hwang

Abstract:

Hydraulic system of excavator gets working energy from hydraulic pump which is connected to output shaft of engine. Recently, main control valve (MCV) which is composed of several independent metering valve (IMV) has been introduced for better energy efficiency of the hydraulic system so that fuel efficiency of the excavator can be improved. Excavator with IMV has 5 operating modes depending on the quantity of regeneration flow. In this system, the hydraulic pump is controlled to supply demanded flow which is needed to operate each mode. Because the regenerated flow supply energy to actuators, the hydraulic pump consumes less energy to make same motion than one that does not regenerate flow. The horse power control is applied to the hydraulic pump of excavator for maintaining engine start under a heavy load and this control makes the flow of hydraulic pump reduced. When excavator is in complex operation such as loading or unloading soil, the hydraulic pump discharges small quantity of working fluid in high pressure. At this operation, the engine of excavator does not run at optimal operating line (OOL). The engine needs to be operated on OOL to improve fuel efficiency and by controlling hydraulic pump the engine can drive on OOL. By continuous mode changing of IMV, the hydraulic pump is controlled to make engine runs on OOL. The simulation result of this study shows that fuel efficiency of excavator with IMV can be improved by considering engine OOL and continuous mode changing algorithm.

Keywords: continuous mode changing, engine fuel consumption, excavator, fuel efficiency, IMV

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2403 Comparison of Visual Acuity Outcome and Complication after Phacoemulsification between Diabetic and Non-Diabetic Patients at Burapha University Hospital, Chonburi, Thailand

Authors: Luksanaporn Krungkraipetch

Abstract:

One hundred cataract patients with phacoemulsification were enrolled in the study to compare of visual acuity outcome and complication after phacoemulsification between diabetic and non-diabetic patients at Burapha University Hospital, Chonburi, Thailand. Fifty patients were diabetic (type II) group and 50 patients were non-diabetic group. All cases were operated by one doctor with the same pre-operative care, operation (phacoemulsification), and post-operative care. Visual acuity and complication after surgery were assessed after the operation for two years. There were no significant differences in demographic data between the two groups. The visual outcome values ≥ 2 lines and ≥ 20/40 had no significant differences between two groups after two years of surgery. The complication rate in diabetic group had cystoid macular edema 16%, rupture posterior capsule 8%, posterior capsule opacity 2%, uveitis 2 %, and 2% endophthalmitis. The non-diabetic group had cystoid macular edema 12%, rupture posterior capsule 8%, uveitis 2%, posterior capsule opacity 2%, and 2% wound leak. Comparison of visual acuity outcome and complication after phacoemulsification between diabetic and non-diabetic patients had no statistical significant differences between these two groups. It was found that cystoid macular edema was the most common complication in both groups and 10% of retinopathy progression was seen.

Keywords: cataract, visual acuity, cataract extraction, phacoemulsification, diabetic retinopathy

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2402 DC Bus Voltage Ripple Control of Photo Voltaic Inverter in Low Voltage Ride-Trough Operation

Authors: Afshin Kadri

Abstract:

Using Renewable Energy Resources (RES) as a type of DG unit is developing in distribution systems. The connection of these generation units to existing AC distribution systems changes the structure and some of the operational aspects of these grids. Most of the RES requires to power electronic-based interfaces for connection to AC systems. These interfaces consist of at least one DC/AC conversion unit. Nowadays, grid-connected inverters must have the required feature to support the grid under sag voltage conditions. There are two curves in these conditions that show the magnitude of the reactive component of current as a function of voltage drop value and the required minimum time value, which must be connected to the grid. This feature is named low voltage ride-through (LVRT). Implementing this feature causes problems in the operation of the inverter that increases the amplitude of high-frequency components of the injected current and working out of maximum power point in the photovoltaic panel connected inverters are some of them. The important phenomenon in these conditions is ripples in the DC bus voltage that affects the operation of the inverter directly and indirectly. The losses of DC bus capacitors which are electrolytic capacitors, cause increasing their temperature and decreasing its lifespan. In addition, if the inverter is connected to the photovoltaic panels directly and has the duty of maximum power point tracking, these ripples cause oscillations around the operating point and decrease the generating energy. Using a bidirectional converter in the DC bus, which works as a buck and boost converter and transfers the ripples to its DC bus, is the traditional method to eliminate these ripples. In spite of eliminating the ripples in the DC bus, this method cannot solve the problem of reliability because it uses an electrolytic capacitor in its DC bus. In this work, a control method is proposed which uses the bidirectional converter as the fourth leg of the inverter and eliminates the DC bus ripples using an injection of unbalanced currents into the grid. Moreover, the proposed method works based on constant power control. In this way, in addition, to supporting the amplitude of grid voltage, it stabilizes its frequency by injecting active power. Also, the proposed method can eliminate the DC bus ripples in deep voltage drops, which cause increasing the amplitude of the reference current more than the nominal current of the inverter. The amplitude of the injected current for the faulty phases in these conditions is kept at the nominal value and its phase, together with the phase and amplitude of the other phases, are adjusted, which at the end, the ripples in the DC bus are eliminated, however, the generated power decreases.

Keywords: renewable energy resources, voltage drop value, DC bus ripples, bidirectional converter

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2401 Analysis of a Multiejector Cooling System in a Truck at Different Loads

Authors: Leonardo E. Pacheco, Carlos A. Díaz

Abstract:

An alternative way of addressing the difficult to recover the useless heat is through an ejector refrigeration cycle for vehicles applications. A group of thermo-compressor supply the mechanical compressor function at conventional refrigeration compression system. The thermo-compressor group recovers the thermal energy from waste streams (exhaust gases product in internal combustion motors, gases burned in wellhead among others) to eliminate the power consumption of the mechanical compressor. These types of alternative cooling system (air-conditioners) present a kind of advantages in both the increase in energy efficiency and the improvement of the COP of the system being studied from their its mechanical simplicity (decrease of moving parts). An ejector refrigeration cycle represents a significant step forward in the optimization of the efficient use of energy in the process of air conditioning and an alternative to reduce the environmental impacts. On one side, with the energy recycling decreases the temperature of the gases thrown into the atmosphere, which contributes to the principal beneficiaries of the average temperature of the planet. In parallel, mitigating the environmental impact caused by the production and handling of conventional cooling fluids commonly available in the market, causing the destruction of the ozone layer. This work had studied the operation of the multiejector cooling system for a truck with a 420 HP engine at different rotation speed. The operation condition limits and the COP of multi-ejector cooling systems applied in a truck are analyzed for a variable rpm range from to 800–1800 rpm.

Keywords: ejector system, exhaust gas, multiejector cooling system, recovery energy

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2400 Local Energy and Flexibility Markets to Foster Demand Response Services within the Energy Community

Authors: Eduardo Rodrigues, Gisela Mendes, José M. Torres, José E. Sousa

Abstract:

In the sequence of the liberalisation of the electricity sector a progressive engagement of consumers has been considered and targeted by sector regulatory policies. With the objective of promoting market competition while protecting consumers interests, by transferring some of the upstream benefits to the end users while reaching a fair distribution of system costs, different market models to value consumers’ demand flexibility at the energy community level are envisioned. Local Energy and Flexibility Markets (LEFM) involve stakeholders interested in providing or procure local flexibility for community, services and markets’ value. Under the scope of DOMINOES, a European research project supported by Horizon 2020, the local market concept developed is expected to: • Enable consumers/prosumers empowerment, by allowing them to value their demand flexibility and Distributed Energy Resources (DER); • Value local liquid flexibility to support innovative distribution grid management, e.g., local balancing and congestion management, voltage control and grid restoration; • Ease the wholesale market uptake of DER, namely small-scale flexible loads aggregation as Virtual Power Plants (VPPs), facilitating Demand Response (DR) service provision; • Optimise the management and local sharing of Renewable Energy Sources (RES) in Medium Voltage (MV) and Low Voltage (LV) grids, trough energy transactions within an energy community; • Enhance the development of energy markets through innovative business models, compatible with ongoing policy developments, that promote the easy access of retailers and other service providers to the local markets, allowing them to take advantage of communities’ flexibility to optimise their portfolio and subsequently their participation in external markets. The general concept proposed foresees a flow of market actions, technical validations, subsequent deliveries of energy and/or flexibility and balance settlements. Since the market operation should be dynamic and capable of addressing different requests, either prioritising balancing and prosumer services or system’s operation, direct procurement of flexibility within the local market must also be considered. This paper aims to highlight the research on the definition of suitable DR models to be used by the Distribution System Operator (DSO), in case of technical needs, and by the retailer, mainly for portfolio optimisation and solve unbalances. The models to be proposed and implemented within relevant smart distribution grid and microgrid validation environments, are focused on day-ahead and intraday operation scenarios, for predictive management and near-real-time control respectively under the DSO’s perspective. At local level, the DSO will be able to procure flexibility in advance to tackle different grid constrains (e.g., demand peaks, forecasted voltage and current problems and maintenance works), or during the operating day-to-day, to answer unpredictable constraints (e.g., outages, frequency deviations and voltage problems). Due to the inherent risks of their active market participation retailers may resort to DR models to manage their portfolio, by optimising their market actions and solve unbalances. The interaction among the market actors involved in the DR activation and in flexibility exchange is explained by a set of sequence diagrams for the DR modes of use from the DSO and the energy provider perspectives. • DR for DSO’s predictive management – before the operating day; • DR for DSO’s real-time control – during the operating day; • DR for retailer’s day-ahead operation; • DR for retailer’s intraday operation.

Keywords: demand response, energy communities, flexible demand, local energy and flexibility markets

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2399 Artificial Insemination for Cattle and Carabaos in Bicol Region, Philippines: Its Implementation and Assessment

Authors: Lourdita Llanto

Abstract:

This study described and assessed the implementation of artificial insemination (AI) for cattle and carabaos in the Bicol Region, Philippines: Albay, Sorsogon and Camarines Sur. Three hundred respondents were interviewed. Results were analyzed using frequency counts, means, percentages and chi-square test. Semen samples from different stations were analyzed for motility, viability and morphology. T-test was used in semen quality evaluation. Provincial AI coordinators (PAIC) were male, averaging 59 years old, married, had college education, served in government service for 34 years, but as PAIC for 5.7 years. All had other designations. Mean AI operation was 11.33 years with annual support from the local government unit of Php76,666.67. AI technicians were males, married, with college education, and trained on AI. Problems were on mobility; inadequate knowledge of farmers in animal raising and AI; and lack of liquid nitrogen and frozen semen supply. There was 2.95 municipalities and breedable cattle/carabaos of 3,091.25 per AI technician. Mean number of artificially inseminated animals per AI technician for 2011 was 28.57 heads for carabaos and 8.64 heads for cattle. There was very low participation rate among farmers. Carabaos were 6.52 years with parity 1.53. Cattle were 5.61 years, with parity of 1.51. Semen quality significantly (p ≤ 0.05) deteriorated in normal and live sperm with storage and handling at the provincial and field stations. Breed, AI technicians practices and AI operation significantly affected conception rate. Mean conception rate was 57.62%.

Keywords: artificial insemination, carabao, parity, mother tanks, frozen semen

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2398 Thermal Securing of Electrical Contacts inside Oil Power Transformers

Authors: Ioan Rusu

Abstract:

In the operation of power transformers of 110 kV/MV from substations, these are traveled by fault current resulting from MV line damage. Defect electrical contacts are heated when they are travelled from fault currents. In the case of high temperatures when 135 °C is reached, the electrical insulating oil in the vicinity of the electrical faults comes into contact with these contacts releases gases, and activates the electrical protection. To avoid auto-flammability of electro-insulating oil, we designed a security system thermal of electrical contact defects by pouring fire-resistant polyurethane foam, mastic or mortar fire inside a cardboard electro-insulating cylinder. From practical experience, in the exploitation of power transformers of 110 kV/MT in oil electro-insulating were recorded some passing disconnecting commanded by the gas protection at internal defects. In normal operation and in the optimal load, nominal currents do not require thermal secure contacts inside electrical transformers, contacts are made at the fabrication according to the projects or to repair by solder. In the case of external short circuits close to the substation, the contacts inside electrical transformers, even if they are well made in sizes of Rcontact = 10‑6 Ω, are subjected to short-circuit currents of the order of 10 kA-20 kA which lead to the dissipation of some significant second-order electric powers, 100 W-400 W, on contact. At some internal or external factors which action on electrical contacts, including electrodynamic efforts at short-circuits, these factors could be degraded over time to values in the range of 10-4 Ω to 10-5 Ω and if the action time of protection is great, on the order of seconds, power dissipation on electrical contacts achieve high values of 1,0 kW to 40,0 kW. This power leads to strong local heating, hundreds of degrees Celsius and can initiate self-ignition and burning oil in the vicinity of electro-insulating contacts with action the gas relay. Degradation of electrical contacts inside power transformers may not be limited for the duration of their operation. In order to avoid oil burn with gas release near electrical contacts, at short-circuit currents 10 kA-20 kA, we have outlined the following solutions: covering electrical contacts in fireproof materials that would avoid direct burn oil at short circuit and transmission of heat from electrical contact along the conductors with heat dissipation gradually over time, in a large volume of cooling. Flame retardant materials are: polyurethane foam, mastic, cement (concrete). In the normal condition of operation of transformer, insulating of conductors coils is with paper and insulating oil. Ignition points of its two components respectively are approximated: 135 °C heat for oil and 200 0C for paper. In the case of a faulty electrical contact, about 10-3 Ω, at short-circuit; the temperature can reach for a short time, a value of 300 °C-400 °C, which ignite the paper and also the oil. By burning oil, there are local gases that disconnect the power transformer. Securing thermal electrical contacts inside the transformer, in cardboard tube with polyurethane foams, mastik or cement, ensures avoiding gas release and also gas protection working.

Keywords: power transformer, oil insulatation, electric contacts, Bucholtz relay

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2397 Identification of Membrane Foulants in Direct Contact Membrane Distillation for the Treatment of Reject Brine

Authors: Shefaa Mansour, Hassan Arafat, Shadi Hasan

Abstract:

Management of reverse osmosis (RO) brine has become a major area of research due to the environmental concerns associated with it. This study worked on studying the feasibility of the direct contact membrane distillation (DCMD) system in the treatment of this RO brine. The system displayed great potential in terms of its flux and salt rejection, where different operating conditions such as the feed temperature, feed salinity, feed and permeate flow rates were varied. The highest flux of 16.7 LMH was reported with a salt rejection of 99.5%. Although the DCMD has displayed potential of enhanced water recovery from highly saline solutions, one of the major drawbacks associated with the operation is the fouling of the membranes which impairs the system performance. An operational run of 77 hours for the treatment of RO brine of 56,500 ppm salinity was performed in order to investigate the impact of fouling of the membrane on the overall operation of the system over long time operations. Over this time period, the flux was observed to have reduced by four times its initial flux. The fouled membrane was characterized through different techniques for the identification of the organic and inorganic foulants that have deposited on the membrane surface. The Infrared Spectroscopy method (IR) was used to identify the organic foulants where SEM images displayed the surface characteristics of the membrane. As for the inorganic foulants, they were identified using X-ray Diffraction (XRD), Ion Chromatography (IC) and Energy Dispersive Spectroscopy (EDS). The major foulants found on the surface of the membrane were inorganic salts such as sodium chloride and calcium sulfate.

Keywords: brine treatment, membrane distillation, fouling, characterization

Procedia PDF Downloads 420
2396 A Study on the Current State and Policy Implications of Engineer Operated National Research Facility and Equipment in Korea

Authors: Chang-Yong Kim, Dong-Woo Kim, Whon-Hyun Lee, Yong-Joo Kim, Tae-Won Chung, Kyung-Mi Lee, Han-Sol Kim, Eun-Joo Lee, Euh Duck Jeong

Abstract:

In the past, together with the annual increase in investment on national R&D projects, the government’s budget investment in FE has steadily maintained. In the case of major developed countries, R&D and its supporting works are distinguished and professionalized in their own right, in so far as having a training system for facilities, equipment operation, and maintenance personnel. In Korea, however, research personnel conduct both research and equipment operation, leading to quantitative shortages of operational manpower and qualitative problems due to insecure employment such as maintenance issues or the loss of effectiveness of necessary equipment. Therefore, the purpose of this study was to identify the current status of engineer operated national research FE in Korea based on a 2017 survey results of domestic facilities and to suggest policy implications. A total of 395 research institutes that carried out national R&D projects and registered more than two FE since 2005 were surveyed on-line for two months. The survey showed that 395 non-profit research facilities were operating 45,155 pieces of equipment with 2,211 engineer operated national research FE, meaning that each engineer had to manage 21 items of FE. Among these, 43.9% of the workers were employed in temporary positions, including indefinite term contracts. Furthermore, the salary and treatment of the engineer personnel were relatively low compared to researchers. In short, engineers who exclusively focused on managing and maintaining FE play a very important role in increasing research immersion and obtaining highly reliable research results. Moreover, institutional efforts and government support for securing operators are severely lacking as domestic national R&D policies are mostly focused on researchers. The 2017 survey on FE also showed that 48.1% of all research facilities did not even employ engineers. In order to solve the shortage of the engineer personnel, the government will start the pilot project in 2012, and then only the 'research equipment engineer training project' from 2013. Considering the above, a national long-term manpower training plan that addresses the quantitative and qualitative shortage of operators needs to be established through a study of the current situation. In conclusion, the findings indicate that this should not only include a plan which connects training to employment but also measures the creation of additional jobs by re-defining and re-establishing operator roles and improving working conditions.

Keywords: engineer, Korea, maintenance, operation, research facilities and equipment

Procedia PDF Downloads 174
2395 Neural Network Supervisory Proportional-Integral-Derivative Control of the Pressurized Water Reactor Core Power Load Following Operation

Authors: Derjew Ayele Ejigu, Houde Song, Xiaojing Liu

Abstract:

This work presents the particle swarm optimization trained neural network (PSO-NN) supervisory proportional integral derivative (PID) control method to monitor the pressurized water reactor (PWR) core power for safe operation. The proposed control approach is implemented on the transfer function of the PWR core, which is computed from the state-space model. The PWR core state-space model is designed from the neutronics, thermal-hydraulics, and reactivity models using perturbation around the equilibrium value. The proposed control approach computes the control rod speed to maneuver the core power to track the reference in a closed-loop scheme. The particle swarm optimization (PSO) algorithm is used to train the neural network (NN) and to tune the PID simultaneously. The controller performance is examined using integral absolute error, integral time absolute error, integral square error, and integral time square error functions, and the stability of the system is analyzed by using the Bode diagram. The simulation results indicated that the controller shows satisfactory performance to control and track the load power effectively and smoothly as compared to the PSO-PID control technique. This study will give benefit to design a supervisory controller for nuclear engineering research fields for control application.

Keywords: machine learning, neural network, pressurized water reactor, supervisory controller

Procedia PDF Downloads 138
2394 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

Procedia PDF Downloads 178
2393 Optimizing Multimodal Teaching Strategies for Enhanced Engagement and Performance

Authors: Victor Milanes, Martha Hubertz

Abstract:

In the wake of COVID-19, all aspects of life have been estranged, and humanity has been forced to shift toward a more technologically integrated mode of operation. Essential work such as Healthcare, business, and public policy are a few notable industries that were initially dependent upon face-to-face modality but have completely reimagined their operation style. Unique to these fields, education was particularly strained because academics, teachers, and professors alike were obligated to shift their curriculums online over the course of a few weeks while also maintaining the expectation that they were educating their students to a similar level accomplished pre-pandemic. This was notable as research indicates two key concepts: Students prefer face-to-face modality, and due to the disruption in academic continuity/style, there was a negative impact on student's overall education and performance. With these two principles in mind, this study aims to inquire what online strategies could be best employed by teachers to educate their students, as well as what strategies could be adopted in a multimodal setting if deemed necessary by the instructor or outside convoluting factors (Such as the case of COVID-19, or a personal matter that demands the teacher's attention away from the classroom). Strategies and methods will be cross-analyzed via a ranking system derived from various recognized teaching assessments, in which engagement, retention, flexibility, interest, and performance are specifically accounted for. We expect to see an emphasis on positive social pressure as a dominant factor in the improved propensity for education, as well as a preference for visual aids across platforms, as research indicates most individuals are visual learners.

Keywords: technological integration, multimodal teaching, education, student engagement

Procedia PDF Downloads 43
2392 Bio-Guided of Active New Alkaloids from Alstonia Brassi Toxicity Antitumour Activity in Silico and Molecular Modeling

Authors: Mesbah Khaled, Bouraoui Ouissal, Benkiniouar Rachid, Belkhiri Lotfi

Abstract:

Alstonia, which are tropical plants with a wide geographical distribution, have been divided into different sections by different authors based on previous studies of several species within the genus. Monachino divides Alstonia into 5 sections, while Pichon divides it into 3 sections. Several plants belonging to this genus, such as Alstonia brassii, have been used in traditional folk medicine to treat ailments such as fever, malaria and dysentery]. Previous studies focusing on the chemical composition of these plants have successfully identified indol alkaloids with cytotoxic, anti-diabetic and anti-inflammatory properties. The newly discovered monomers are structurally similar to the backbones of picralin, affinisin and macrolin. On the other hand, all recently isolated dimeric compounds have a macrolin moiety. In this study, a computational analysis was performed on a series of novel molecules, including both monomeric and dimeric compounds with different structural frameworks. This investigation represents the first computational study of these molecules using an in silico approach incorporating 2D-QSAR data. The analysis involved various computational techniques, including 2D-QSAR modelling, molecular docking studies and subsequent validation by molecular dynamics simulation and assessment of ADMET properties. The chemical composition was identified by 1D and 2D NMR. Eight new alkaloids were isolated, 5 monomers and 3 dimers. In this section, we focus on the biological activity of 4 new alkaloids belonging to two different skeletons, the affinisine skeleton.

Keywords: affinisine, talcarpine, macroline, cytotoxicity, alkaloids

Procedia PDF Downloads 256
2391 Organotin (IV) Based Complexes as Promiscuous Antibacterials: Synthesis in vitro, in Silico Pharmacokinetic, and Docking Studies

Authors: Wajid Rehman, Sirajul Haq, Bakhtiar Muhammad, Syed Fahad Hassan, Amin Badshah, Muhammad Waseem, Fazal Rahim, Obaid-Ur-Rahman Abid, Farzana Latif Ansari, Umer Rashid

Abstract:

Five novel triorganotin (IV) compounds have been synthesized and characterized. The tin atom is penta-coordinated to assume trigonal-bipyramidal geometry. Using in silico derived parameters; the objective of our study is to design and synthesize promiscuous antibacterials potent enough to combat resistance. Among various synthesized organotin (IV) complexes, compound 5 was found as potent antibacterial agent against various bacterial strains. Further lead optimization of drug-like properties was evaluated through in silico predictions. Data mining and computational analysis were utilized to derive compound promiscuity phenomenon to avoid drug attrition rate in designing antibacterials. Xanthine oxidase and human glucose- 6-phosphatase were found as only true positive off-target hits by ChEMBL database and others utilizing similarity ensemble approach. Propensity towards a-3 receptor, human macrophage migration factor and thiazolidinedione were found as false positive off targets with E-value 1/4> 10^-4 for compound 1, 3, and 4. Further, displaying positive drug-drug interaction of compound 1 as uricosuric was validated by all databases and docked protein targets with sequence similarity and compositional matrix alignment via BLAST software. Promiscuity of the compound 5 was further confirmed by in silico binding to different antibacterial targets.

Keywords: antibacterial activity, drug promiscuity, ADMET prediction, metallo-pharmaceutical, antimicrobial resistance

Procedia PDF Downloads 487
2390 Insight into the Binding Theme of CA-074Me to Cathepsin B: Molecular Dynamics Simulations and Scaffold Hopping to Identify Potential Analogues as Anti-Neurodegenerative Diseases

Authors: Tivani Phosa Mashamba-Thompson, Mahmoud E. S. Soliman

Abstract:

To date, the cause of neurodegeneration is not well understood and diseases that stem from neurodegeneration currently have no known cures. Cathepsin B (CB) enzyme is known to be involved in the production of peptide neurotransmitters and toxic peptides in neurodegenerative diseases (NDs). CA-074Me is a membrane-permeable irreversible selective cathepsin B (CB) inhibitor as confirmed by in vivo studies. Due to the lack of the crystal structure, the binding mode of CA-074Me with the human CB at molecular level has not been previously reported. The main aim of this study is to gain an insight into the binding mode of CB CA-074Me to human CB using various computational tools. Herein, molecular dynamics simulations, binding free energy calculations and per-residue energy decomposition analysis were employed to accomplish the aim of the study. Another objective was to identify novel CB inhibitors based on the structure of CA-074Me using fragment based drug design using scaffold hoping drug design approach. Results showed that two of the designed ligands (hit 1 and hit 2) were found to have better binding affinities than the prototype inhibitor, CA-074Me, by ~2-3 kcal/mol. Per-residue energy decomposition showed that amino acid residues Cys29, Gly196, His197 and Val174 contributed the most towards the binding. The Van der Waals binding forces were found to be the major component of the binding interactions. The findings of this study should assist medicinal chemist towards the design of potential irreversible CB inhibitors.

Keywords: cathepsin B, scaffold hopping, docking, molecular dynamics, binding-free energy, neurodegerative diseases

Procedia PDF Downloads 359
2389 Towards an African Model: A Survey of Social Enterprises in South Africa

Authors: Kerryn Krige, Kerrin Myers

Abstract:

Social entrepreneurship offers the opportunity to simultaneously address both social and economic inequality in South Africa. Its appeal across racial groups, its attractiveness to young people, its applicability in rural and peri-urban markets, and its acceleration in middle income, large-business economies suits the South African context. However, the potential to deliver much-needed developmental benefits has not been realised because the social entrepreneurship debate lacks evidence as to who social entrepreneurs are, their goals and operations and the socio-economic results they achieve. As a result, policy development has been stunted, and legislative barriers and red tape remain. Social entrepreneurs are isolated from the mainstream economy, and struggle to access funding because of limitations in legislative and organisational structures. The objective of the study is to strengthen the ecosystem for social entrepreneurship in South Africa by producing robust, policy-rich information from and about social enterprises currently in operation across the country. The study employs a quantitative survey methodology, using online and telephonic data collection methods. A purposive sample of 1000 social enterprises was included in the first large-scale study of social entrepreneurship in South Africa. The results offer deep insight into the characteristics of social enterprises; the activities they undertake and the markets they serve; their modes of operation and funding sources as well as key challenges and support systems. The results contribute towards developing a model of social enterprise in the African context.

Keywords: social enterprise, key characteristics, challenges and enablers, towards an African model

Procedia PDF Downloads 287
2388 Agritourism Development Mode Study in Rural Area of Boshan China

Authors: Lingfei Sun

Abstract:

Based on the significant value of ecology, the strategic planning for ecological civilization construction was mentioned in the 17th and 18th National Congress of the Communist Party of China. How to generate economic value based on the environmental capacity is not only an economic decision but also a political decision to make. Boshan took the full use of “Ecology” and transformed it as an inexhaustible green resource to benefit people, reflecting the sustainable value of new agriculture development mode. The Strawberry Harvest Festival and Blueberry Harvest Festival hosted approximately 96,000 and 54,000 leisure tourists respectively in 2014. For the Kiwi Harvest Festival in August 2014, in average, it attracted about 4600 tourists per day, which generated daily kiwi sales of 50,000 lbs and 3 million RMB (About 476,000 USD) of daily revenue. The purpose of this study is to elaborate the modes of agritourism development, by analyzing the cases in rural area of Boshan, China. Interviews with the local government officers were applied to discover operation mode of agritourism operation. The financial data was used to demonstrate the strength of government policy and improvement of the income of rural people. The result indicated that there are mainly three types of modes: the Intensive Mode, the Model Mode and the Mixed Mode, supported by case study respectively. With the boom of tourism, the development of agritourism in Boshan relies on the agriculture encouraging policy of China and the effort of local government; meanwhile, large scale of cultivation and the product differentiation are the crucial elements for the success of rural agritourism projects.

Keywords: agriculture, agritourism, economy, rural area development

Procedia PDF Downloads 288
2387 Computational Investigation of V599 Mutations of BRAF Protein and Its Control over the Therapeutic Outcome under the Malignant Condition

Authors: Mayank, Navneet Kaur, Narinder Singh

Abstract:

The V599 mutations in the BRAF protein are extremely oncogenic, responsible for countless of malignant conditions. Along with wild type, V599E, V599D, and V599R are the important mutated variants of the BRAF proteins. The BRAF inhibitory anticancer agents are continuously developing, and sorafenib is a BRAF inhibitor that is under clinical use. The crystal structure of sorafenib bounded to wild type, and V599 is known, showing a similar interaction pattern in both the case. The mutated 599th residue, in both the case, is also found not interacting directly with the co-crystallized sorafenib molecule. However, the IC50 value of sorafenib was found extremely different in both the case, i.e., 22 nmol/L for wild and 38 nmol/L for V599E protein. Molecular docking study and MMGBSA binding energy results also revealed a significant difference in the binding pattern of sorafenib in both the case. Therefore, to explore the role of distinctively situated 599th residue, we have further conducted comprehensive computational studies. The molecular dynamics simulation, residue interaction network (RIN) analysis, and residue correlation study results revealed the importance of the 599th residue on the therapeutic outcome and overall dynamic of the BRAF protein. Therefore, although the position of 599th residue is very much distinctive from the ligand-binding cavity of BRAF, still it has exceptional control over the overall functional outcome of the protein. The insight obtained here may seem extremely important and guide us while designing ideal BRAF inhibitory anticancer molecules.

Keywords: BRAF, oncogenic, sorafenib, computational studies

Procedia PDF Downloads 103
2386 A Power Management System for Indoor Micro-Drones in GPS-Denied Environments

Authors: Yendo Hu, Xu-Yu Wu, Dylan Oh

Abstract:

GPS-Denied drones open the possibility of indoor applications, including dynamic arial surveillance, inspection, safety enforcement, and discovery. Indoor swarming further enhances these applications in accuracy, robustness, operational time, and coverage. For micro-drones, power management becomes a critical issue, given the battery payload restriction. This paper proposes an application enabling battery replacement solution that extends the micro-drone active phase without human intervention. First, a framework to quantify the effectiveness of a power management solution for a drone fleet is proposed. The operation-to-non-operation ratio, ONR, gives one a quantitative benchmark to measure the effectiveness of a power management solution. Second, a survey was carried out to evaluate the ONR performance for the various solutions. Third, through analysis, this paper proposes a solution tailored to the indoor micro-drone, suitable for swarming applications. The proposed automated battery replacement solution, along with a modified micro-drone architecture, was implemented along with the associated micro-drone. Fourth, the system was tested and compared with the various solutions within the industry. Results show that the proposed solution achieves an ONR value of 31, which is a 1-fold improvement of the best alternative option. The cost analysis shows a manufacturing cost of $25, which makes this approach viable for cost-sensitive markets (e.g., consumer). Further challenges remain in the area of drone design for automated battery replacement, landing pad/drone production, high-precision landing control, and ONR improvements.

Keywords: micro-drone, battery swap, battery replacement, battery recharge, landing pad, power management

Procedia PDF Downloads 91
2385 Assessment of Isatin as Surface Recognition Group: Design, Synthesis and Anticancer Evaluation of Hydroxamates as Novel Histone Deacetylase Inhibitors

Authors: Harish Rajak, Kamlesh Raghuwanshi

Abstract:

Histone deacetylase (HDAC) are promising target for cancer treatment. The panobinostat (Farydak; Novartis; approved by USFDA in 2015) and chidamide (Epidaza; Chipscreen Biosciences; approved by China FDA in 2014) are the novel HDAC inhibitors ratified for the treatment of patients with multiple myeloma and peripheral T cell lymphoma, respectively. On the other hand, two other HDAC inhibitors, Vorinostat (SAHA; approved by USFDA in 2006) and Romidepsin (FK228; approved by USFDA in 2009) are already in market for the treatment of cutaneous T-cell lymphoma. Several hydroxamic acid based HDAC inhibitors i.e., belinostat, givinostat, PCI24781 and JNJ26481585 are in clinical trials. HDAC inhibitors consist of three pharmacophoric features - an aromatic cap group, zinc binding group (ZBG) and a linker chain connecting cap group to ZBG. Herein, we report synthesis, characterization and biological evaluation of HDAC inhibitors possessing substituted isatin moiety as cap group which recognize the surface of active enzyme pocket and thiosemicarbazide moiety incorporated as linker group responsible for connecting cap group to ZBG (hydroxamic acid). Several analogues were found to inhibit HDAC and cellular proliferation of Hela cervical cancer cells with GI50 values in the micro molar range. Some of the compounds exhibited promising results in vitro antiproliferative studies. Attempts were also made to establish the structure activity relationship among synthesized HDAC inhibitors.

Keywords: HDAC inhibitors, hydroxamic acid derivatives, isatin derivatives, antiproliferative activity, docking

Procedia PDF Downloads 295