Search results for: selective serotonin reuptake inhibitors (SSRIs)

Authors: N. K. Thakur

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A major proportion of the formations drilled for the production of hydrocarbons consists of clay containing shales. The petroleum industry has hugely investigated the role of clay minerals and their subsequent effect on wellbore stability during the drilling and production of hydrocarbons. It has been found that when the shale formation comes in contact with water-based drilling fluid, the interaction of clay minerals like montmorillonite with infiltrated water leads to hydration of the clay minerals, which causes shale swelling. When shale swelling proceeds further, it may lead to major drilling complications like caving, pipe sticking, which invariably influences wellbore stability, wellbore diameter, the mechanical strength of shale, stress distribution in the wellbore, etc. These problems ultimately lead to an increase in nonproductive time and additional costs during drilling. Several additives are used to prevent shale instability. Among the popular additives used for shale inhibition in drilling muds, ionic liquids and nanoparticles are emerging to be the best additives. The efficiency of the proposed additives will be studied and compared with conventional clay inhibitors like KCl. The main objective is to develop a highly efficient water-based mud for mitigating shale instability and reducing fluid loss which is environmentally friendly and does not alter the formation permeability. The use of nanoparticles has been exploited to enhance the rheological and fluid loss properties in water-based drilling fluid ionic liquid have attracted significant research interest due to its unique thermal stability. It is referred to as ‘green chemical’. The preliminary experimental studies performed are promising. The application of more effective mud additives is always desirable to make the drilling process techno-economically proficient.

Keywords: ionic liquid, shale inhibitor, wellbore stability, unconventional

Procedia PDF Downloads 166

Authors: C. Iraklis, G. Evmiridis, A. Iraklis

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Renewable energy sources and distributed power generation units already have an important role in electrical power generation. A mixture of different technologies penetrating the electrical grid, adds complexity in the management of distribution networks. High penetration of distributed power generation units creates node over-voltages, huge power losses, unreliable power management, reverse power flow and congestion. This paper presents an optimization algorithm capable of reducing congestion and power losses, both described as a function of weighted sum. Two factors that describe congestion are being proposed. An upgraded selective particle swarm optimization algorithm (SPSO) is used as a solution tool focusing on the technique of network reconfiguration. The upgraded SPSO algorithm is achieved with the addition of a heuristic algorithm specializing in reduction of power losses, with several scenarios being tested. Results show significant improvement in minimization of losses and congestion while achieving very small calculation times.

Keywords: congestion, distribution networks, loss reduction, particle swarm optimization, smart grid

Procedia PDF Downloads 422

Authors: A. Yongsheng Guo, B. Obedat. Abdulazeez, C. Xiaoxian Zhu

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This study aimed to identify the barriers to the development of small and medium-sized enterprises (SMEs) in China and build a theoretical framework to evaluate the support provided by the authorities and institutions. A grounded theory approach was adopted to collect and analyze data. 32 interviews were conducted with SME managers, and open, axial and selective coding was utilized to develop themes. Based on institutional theory, grounded theory models were used to present findings. The findings showed that the main barriers in the business environment were defaulting on contracts, bureaucracy in procedures, lack of financial and legal support, limited intermediaries and channels, and poor quality of products and services. This study found that many programs were provided to support SMEs. A theoretical framework was developed to evaluate the performance of the programs from the managers’ perspective. The concepts of economy, efficiency and effectiveness were used to evaluate the perceived value of the programs. This study suggests that specialized programs are needed to suit sector-specific requirements, and creative packages are helpful in supporting SMEs' growth.

Keywords: business support, public economics, public programme, SME

Procedia PDF Downloads 18

Authors: Meral Tuncbilek, Duygu Sac, Irem Durmaz, Rengul Cetin Atalay

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Nucleoside analogs are a pharmacologically diverse family that includes cytotoxic compounds, antiviral agents, and immunosuppressive molecules. Purine nucleoside derivatives such as fludarabine, cladribine, and pentostatin are significant drugs used in chemotherapy for the treatment of solid tumors and hematological malignancies. In this study, we synthesized novel purine ribonucleoside analogs containing a 4-(4-substituted phenylsulfonyl) piperazine in the substituent at N6- and O-substituted sulfonyl group at 5’-position as putative cytotoxic agents. The newly obtained compounds were then characterized for their cytotoxicity in human cancer cell lines. The 5’, 6-disubstituted 9-(β-D-ribofuranosyl)purine derivatives (44-67) were readily obtained from commercially available inosine in seven steps in very cost effective synthesis approach. The newly synthesized compounds were first evaluated for their anti-tumor activities against human liver (Huh7), colon (HCT116) and breast (MCF7) carcinoma cell lines. The IC50 values were in micromolar concentrations with 5’, 6-disubstituted purine nucleoside derivatives. Time-dependent IC50 values for each molecule were also calculated in comparison with known cytotoxic agents Camptothecin (CPT), 5-Fluorouracil (5-FU), Cladribine, Pentostatine and Fludarabine. N6-(4-trifluoromethyl phenyl) / N6-(4-bromophenyl) and 5’-O-(4-methoxybenzene sulfonyl) / 5’-O-(benzenesulfonyl) derivatives 54, 64 displayed the best cytotoxic activity with IC50 values of 8.8, 7 µM against MCF7 cell line. The N6-(4-methylphenyl) analog 50 was also very active (IC50= 10.7 μM) against HCT116 cell line. Furthermore, compound 64 had a better cytotoxic activity than the known cell growth inhibitors 5-FU and Fludarabine on Huh7 (1.5 vs 30.7, 29.9 μM for 5-FU and Fludarabine).

Keywords: cytotoxic activity, Huh7, HCT116, MCF7, nucleoside, synthesis

Procedia PDF Downloads 224

Authors: Heba Kamal Mohamed

Abstract:

Introduction: Tramadol is a weak -opioid receptor agonist with an analgesic effect because of the inhibition of uptake of norepinephrine and serotonin. Nowadays, tramadol hydrochloride is frequently used as a pain reliever. Tramadol is recommended for the management of acute and chronic pain of moderate to severe intensity associated with a variety of diseases or problems, including osteoarthritis, diabetic neuropathy, neuropathic pain, and even perioperative pain in human patients. In obstetrics and gynecology, tramadol is used extensively to treat postoperative pain. Aim of the study: This study was undertaken to investigate the histological (light and electron microscopic) and immunohistochemical effects of long term tramadol treatment on the ovary of adult rats and the possible recovery after tramadol withdrawal. Design: Experimental study. Materials and methods: Thirty adult female albino rats were used in this study. They were classified into three main groups (10 rats each). Group I served as the control group. Group II, rats were subcutaneously injected with tramadol 40 mg/kg three times per week for 8 weeks. Group III, rats were subcutaneously injected with tramadol 40 mg/kg three times per week for 8 weeks then were kept for another 8 weeks without treatment for recovery. At the end of the experiment rats were sacrificed and bilateral oophorectomy was carried out; the ovaries were processed for histological study (light and electron microscopic) and immunohistochemical reaction for caspase-3 (apoptotic protein). Results: Examination of the ovary of tramadol-treated rats (group II) revealed many atretic ovarian follicles, some follicles showed detachment of the oocyte from surrounding granulosa cells and others showed loss of the oocyte. Many follicles revealed degenerated vacuolated oocytes and vacuolated theca folliculi cells. Granulosa cells appeared shrunken, disrupted and loosely attached with vacuolated cytoplasm and pyknotic nuclei. Some follicles showed separation of granulosa cells from the theca folliculi layer. The ultrastructural study revealed the presence of granulosa cells with electron dense indented nuclei, damaged mitochondria and granular vacuolated cytoplasm. Other cells showed accumulation of large amount of lipid droplets in their cytoplasm. Some follicles revealed rarifaction of the cytoplasm of oocytes and absent zona pellucida. Moreover, apoptotic changes were detected by immunohistochemical staining in the form of increased staining intensity to caspase-3 (apoptotic protein). With Masson's Trichrome stain, there was an increased collagen fibre deposition in the ovarian cortical stroma. The wall of blood vessels appeared thickened. In the withdrawal group (group III), there was a little improvement in the histological and immunohistochemical changes. Conclusion: Tramadol had serious deleterious effects on ovarian structure. Thus, it should be used with caution, especially when a long term treatment is indicated. Withdrawal of tramadol led to a little improvement in the structural impairment of the ovary.

Keywords: tramadol, ovary, withdrawal, rats

Procedia PDF Downloads 273

Authors: Said Belaaouad

Abstract:

This study aimed to explore the quantitative structure-activity relationship (QSAR) of 1,2,4-Triazine-3(2H)-one derivative as a potential anticancer agent against breast cancer. The electronic descriptors were obtained using the Density Functional Theory (DFT) method, and a multiple linear regression techniques was employed to construct the QSAR model. The model exhibited favorable statistical parameters, including R2=0.849, R2adj=0.656, MSE=0.056, R2test=0.710, and Q2cv=0.542, indicating its reliability. Among the descriptors analyzed, absolute electronegativity (χ), total energy (TE), number of hydrogen bond donors (NHD), water solubility (LogS), and shape coefficient (I) were identified as influential factors. Furthermore, leveraging the validated QSAR model, new derivatives of 1,2,4-Triazine-3(2H)-one were designed, and their activity and pharmacokinetic properties were estimated. Subsequently, molecular docking (MD) and molecular dynamics (MD) simulations were employed to assess the binding affinity of the designed molecules. The Tubulin colchicine binding site, which plays a crucial role in cancer treatment, was chosen as the target protein. Through the simulation trajectory spanning 100 ns, the binding affinity was calculated using the MMPBSA script. As a result, fourteen novel Tubulin-colchicine inhibitors with promising pharmacokinetic characteristics were identified. Overall, this study provides valuable insights into the QSAR of 1,2,4-Triazine-3(2H)-one derivative as potential anticancer agent, along with the design of new compounds and their assessment through molecular docking and dynamics simulations targeting the Tubulin-colchicine binding site.

Keywords: QSAR, molecular docking, ADMET, 1, 2, 4-triazin-3(2H)-ones, breast cancer, anticancer, molecular dynamic simulations, MMPBSA calculation

Procedia PDF Downloads 69

Authors: Dong-Gyu Leem, Ji-Sun Shin, Sang Yoon Choi, Kyung-Tae Lee

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In this study, we focused on the anti-proliferative effects of panaxydol, a C17 polyacetylenic compound derived from Panax ginseng roots, against various human cancer cells. We treated with panaxydol to various cancer cells and panaxydol treatment was found to significantly inhibit the proliferation of human lung cancer cells (A549) and human pancreatic cancer cells (AsPC-1 and MIA PaCa-2), of which AsPC-1 cells were most sensitive to its treatment. DNA flow cytometric analysis indicated that panaxydol blocked cell cycle progression at the G1 phase in A549 cells, which accompanied by a parallel reduction of protein expression of cyclin-dependent kinase (CDK) 2, CDK4, CDK6, cyclin D1 and cyclin E. CDK inhibitors (CDKIs), such as p21CIP1/WAF1 and p27KIP1, were gradually upregulated after panaxydol treatment at the protein levels. Furthermore, panaxydol induced the activation of p53 in A549 cells. In addition, panaxydol also induced apoptosis of AsPC-1 and MIA PaCa-2 cells, as shown by accumulation of subG1 and apoptotic cell populations. Panaxydol triggered the activation of caspase-3, -8, -9 and the cleavage of poly (ADP-ribose) polymerase (PARP). Reduction of mitochondrial transmembrane potential by panaxydol was determined by staining with dihexyloxacarbocyanine iodide. Furthermore, panaxydol suppressed the levels of anti-apoptotic proteins, XIAP and Bcl-2, and increased the levels of proapoptotic proteins, Bax and Bad. In addition, panaxydol inhibited the activation of Akt and extracellular signal-regulated kinase (ERK) and activated the p38 mitogen-activated protein kinase kinase (MAPK). Our results suggest that panaxydol is an anti-tumor compound that causes p53-mediated cell cycle arrest and apoptosis via mitochondrial apoptotic pathway in various cancer cells.

Keywords: apoptosis, cancer, G1 arrest, panaxydol

Procedia PDF Downloads 303

Authors: A. H. Tadevosyan, S. K. Mayrapetyan, N. B. Tavakalyan, K. I. Pyuskyulyan, A. H. Hovsepyan, S. N. Sergeeva

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Soil contamination with radiocesium has a long-term radiological impact due to its long physical half-life (30.1 years for 137Cs and 2 years for 134Cs) and its high biological availability. 137Cs causes the largest concerns because of its deleterious effect on agriculture and stock farming, and, thus, human life for decades. One of the important aspects of the problem of contaminated soils remediation is understand of protective actions aimed at the reduction of biological migration of radionuclides in soil-plant system. The most effective way to bind radionuclides is the use of selective sorbents. The proposed research mainly aims to achieve control on transfer of 137Cs in a system growing media–plant due to counter ions variation in the polymeric sorbents. As the research object, Japanese basil-Perilla frutescens was chosen. Productivity of plants depending on the presence (control-without presence of polymer) and type of polymer material, as well as content of 137Cs in plant material has been determined. The character of different polymers influences on the 137Cs migration in growing media–plant system as well as accumulation in the plants has been cleared up.

Keywords: radioceaseum, Japanese basil, polymer, soil-plant system

Procedia PDF Downloads 169

Authors: David Downey

Abstract:

With the introduction of additive manufacturing (3D printing) to produce titanium (Ti6Al4V) components in the medical/aerospace and automotive industries, intricate geometries can be produced with virtually complete design freedom. However, the consideration of microstructural anisotropy resulting from the additive manufacturing process becomes necessary due to this design flexibility and the need to print a geometric shape that can consist of numerous angles, radii, and swept surfaces. A femoral knee implant serves as an example of a 3D-printed near-net-shaped product. The mechanical properties of the printed components, and consequently, their machinability, are affected by microstructural anisotropy. Currently, finish-machining operations performed on titanium printed parts using selective laser melting (SLM) utilize the same cutting tools employed for processing wrought titanium components. Cutting forces for components manufactured through SLM can be up to 70% higher than those for their wrought counterparts made of Ti6Al4V. Moreover, temperatures at the cutting interface of 3D printed material can surpass those of wrought titanium, leading to significant tool wear. Although the criteria for tool wear may be similar for both 3D printed and wrought materials, the rate of wear during the machining process may differ. The impact of these issues on the choice of cutting tool material and tool lifetimes will be discussed.

Keywords: additive manufacturing, build orientation, microstructural anisotropy, printed titanium Ti6Al4V, tool wear

Procedia PDF Downloads 73

Authors: Hamid Hossein Khezri, Afsaneh Javdani-Mallak

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Fast inhibitory neurotransmission in the mammalian nervous system is largely mediated by GABAA receptors, chloride-selective members of the superfamily of pentameric Cys-loop receptors. Cannabidiol (CBD) is one of the members of cannabinoid compounds found in cannabis. CBD and Cannabinol (CBN), as the other extract of plant Cannabis were able to reduce myofascial pain in rats with immunosuppressive and anti-inflammatory activities. In this study, we accomplished protein-protein BLAST, and the sequence was found to be for Gamma-aminobutyric acid receptor subunit alpha-1 (GBRA1) chain A and its 3D structure was subsequently downloaded from Protein Data Bank. The structures of the ligands, cannabinol, and cannabidiol, were obtained from PubChem. After the necessary process of the obtained files, AutoDock Vina was used to perform molecular docking. Docking between the ligands and GBRA1 chain A revealed that cannabinol has a higher affinity to GBRA1 (binding energy = -7.5 kcal/mol) compared to cannabidiol (binding energy = -6.5 kcal/mol). Furthermore, cannabinol seems to be able to interact with 10 residues of the protein, out of which 3 are in the neurotransmitter-gated ion-channel transmembrane domain of GBRA1, whereas cannabidiol interacts with two other residues. Although the results of this project do not indicate the activating /or inhibitory capability of the studied compounds, it suggests that cannabinol can act as a relatively strong ligand for GBRA1.

Keywords: protein-ligand docking, cannabinol, cannabidiol, GBRA1

Procedia PDF Downloads 94

Authors: Ikediobi Lottanna Samuel

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Days are gone when perpetrators of core international crimes hide under the cloak of sovereignty to go with impunity. The principle of international criminal responsibility is a reality. This move to end impunity for violation of human rights has led to the creation of international and hybrid tribunals, a permanent international criminal court, and increased prosecution of human rights violations in domestic courts. This article examines the attempts by the international community to bring perpetrators of heinous crimes to book. The work reveals the inadequacy of the current international mechanism for prosecuting core international crimes in order to end the culture of impunity and entrench the culture of accountability. It also identifies that ad hoc international criminal tribunals and the international criminal court face similar challenges ranging from lack of cooperation by nation states, non-existence of hierarchy of crimes, lack of effective enforcement mechanism, limited prosecutorial capacity and agenda, difficulty in apprehending suspects, difficulty in blending different legal tradition, absence of a coherent sentencing guideline, distant location of courts, selective indictment, etc. These challenges adversely affect the functioning of these courts. It is suggested that a more helpful way to end impunity would be to have a more robust and synergistic relationship between national, regional, and international approaches to prosecuting core international crimes.

Keywords: prosecution, criminal, international, tribunal, justice, ad hoc

Procedia PDF Downloads 194

Authors: Rizalyn Gonzales, Harold Monteclaro

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This study determined the effects of net height on the capture performance of crab entangling nets. Fishing trials were conducted using nets with the following net heights: 1) 12 meshes down (MD), 2) 24 MD and 3) 50 MD. A total of 1,290 individuals comprising of 87 species belonging to 53 families were caught. One-way ANOVA showed that net height significantly affects various catch parameters such as catch per unit effort (CPUE) of the total and target catch, amount of non-target catch, sizes and species richness. The use of appropriate net height is a potential technical measure for a selective but still efficient crab entangling net fishery. Lower net height significantly reduced non-target catch up to 70%. While lower nets decreased the CPUE of target catch such as blue swimming crab Portunus pelagicus and christian crab Charybdis feriatus up to 65% in 12 MD, catch in 24 MD was not significantly different with that in 50 MD. The use of 24 MD also resulted in capturing larger-sized Portunus pelagicus. Catch species richness decreased up to 58% in lower nets. These results are useful to fisheries managers and government institutions to develop or improve existing regulations towards a sustainable crab fishery particularly blue swimming crabs.

Keywords: blue swimming crabs, catch per unit effort, crab entangling nets, net height

Procedia PDF Downloads 203

Authors: Samira Kilani-Morakchi, Amina Badi, Nadia Aribi

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German cockroach, Blattella germanica, is known to be an important pest due to its high reproductive potential and its ability to build up large infectious populations. The infestations were generally controlled by neurotoxic insecticides including organophosphates (OP), carbamate and pyrethroids. An alternative cockroach’s control approach is the use insect growth regulators (IGRs). The relative fewer effects of these chemicals on non-target insects and animals, and their favourable environmental fate, make them attractive insecticides for inclusion in integrated pest management programmes. The juvenoids and chitin synthesis inhibitors are two classes of IGRs that have received the most attention for useful chemicals to manage German cockroaches while ecdysone agonists were mostly used to control Lepidopteran species. In the present study, the sublethal effects of the non-sreroidal ecdysone agonist tebufenozide were evaluated topically on adults of the B. germanica. The effects on reproduction were observed in adults females of cockroaches that survived exposure to LD25 (146 µg/g of insect) of tebufenozide. Dissection of treated females showed a clear reduction in both the number of oocytes per paired ovaries and the size of basal oocytes, as compared to controls. In addition, tebufenozide significantly reduced the mating success of pairs and altered the fertility as shown through the reduction of ootheca development and total absence of viable nymph. Tebufenozide disrupted the German cockroach reproduction by interfering with homeostasis of the insect hormones. In conclusion, the overall results suggested that tebufenozide can be used as a biorational insecticide for controlling cockroaches.

Keywords: B. germanica, ecdysteroid agonist, tebufenozide, reproduction

Procedia PDF Downloads 276

Authors: Franciele G. Esteves, Jose R. A. dos Santos-Pinto, Caroline L. de Souza, Mario S. Palma

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Orb-weaving spiders use a very strong, stickiness, and elastic web to catch the prey. These web properties would be enough for the entrapment of prey; however, these spiders may be hiding venomous secrets on the web, which are being revealed now. Here we provide strong proteome, peptidome, and transcriptomic evidence for the presence of toxic components on the web silk from Nephila clavipes. Our scientific outcomes revealed, both in the web silk and in the silk-producing glands, a wide diversity of toxins/neurotoxins, defensins, and proteolytic enzymes. These toxins/neurotoxins are similar to toxins isolated from animal venoms, such as Sphigomyelinase D, Latrotoxins, Zodatoxins, Ctenitoxin Pn and Pk, Agatoxins and Theraphotoxin. Moreover, the insect-toxicity results with the web silk crude extract demonstrated that these toxic components can be lethal and/or cause paralytic effects to the prey. Therefore, through OMICs approaches, the results presented until now may contribute to a better understanding of the chemical and ecological interaction of these compounds in insect-prey capture by spider web N. clavipes, demonstrating that the web is not only a simple mechanical tool but has a chemical-active involvement in prey capture. Moreover, the results can also contribute to future studies of possible development of a selective insecticide or even in possible pharmacological applications.

Keywords: web silk toxins, silk-produncing glands, de novo transcriptome assembly, LCMS-based proteomics

Procedia PDF Downloads 116

Authors: Z. Miao, Y. Chu, Y. Zhang

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The unique cholesteric phase liquid crystals obtained by mixing nematic liquid crystals with chiral dopants have gained valuable applications in the display field for their selective reflection and circular dichroism properties. The periodic arrangement of the helical structure of cholesteric liquid crystals makes it possible to produce Bragg reflection of circularly polarized light irradiated perpendicularly to the liquid crystals and, therefore, to acquire semi- or fully reflective surfaces or films. If the polymer-liquid crystal composites are combined with polymeric monomers, commercialized reflective broadband films can be fabricated. In this study, the polymer-liquid crystal composites reflecting visible light region (wavelength centered at 550 nm) were studied to analyze the effects of AC electric field at different voltages and frequencies on the optical texture of the composites, as well as the effects of polymerization temperature and ultraviolet (UV) intensity on the polymerization reaction and reflection bandwidth. The optimal sample was finally obtained at 100Hz, 120V, 30℃, 1.00 mW/cm², which provides a research suggestion to solve the influencing factors of visible light reflection bandwidths.

Keywords: cholesteric liquid crystal, reflection bandwidths, negative dielectric anisotropy, planar texture

Procedia PDF Downloads 143

Authors: Liang Ning, Chung Hau Yin

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Angiogenesis is the process of new blood vessel development. It has been recognized as a therapeutic target for blocking cancer growth four decades ago. Vascular sprouting is initiated by pro-angiogenic factors. Vascular endothelial cell growth factor (VEGF) plays a central role in angiogenic initiation, many patients with cancer or ocular neovascularization have been benefited from anti-VEGF therapy. Emerging approaches impacting in the later stages of vessel remodeling and maturation are expected to improve clinical efficacy. TIE receptor as well as the corresponding angiopoietin ligands, were identified as another endothelial cell specific receptor tyrosine kinase signaling system. Much efforts were made to reduce the activity of angiopoietin-TIE receptor axis. Two eudesmane-type sesquiterpenes from laggera alata, namely, 15-dihydrocostic acid and ilicic acid were found with strong anti-angiogenic properties in zebrafish model. Meanwhile, the mRNA expression levels of VEGFR2 and TIE2 pathway related genes were down-regulated in the sesquiterpenes treated zebrafish embryos. Besides, in human umbilical vein endothelial cells (HUVECs), the sesquiterpenes have the ability to inhibit VEGF-induced HUVECs proliferation and migration at non-toxic concentration. Moreover, angiopoietin-2 induced TIE2 phosphorylation was inhibited by the sesquiterpenes, the inhibitory effect was detected in angiopoietin-1 induced HUVECs proliferation as well. Thus, we hypothesized the anti-angiogenic activity of the compounds may via the inhibition of VEGF and TIE2 related pathways. How the compounds come into play as the pathways inhibitors need to be evaluated in the future.

Keywords: Laggera alata, eudesmane-type sesquiterpene, anti-angiogenesis, VEGF, angiopoietin, TIE2

Procedia PDF Downloads 187

Authors: Syed Khurram Mahmud, Athar Naveed, Shoaib Arif

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Beamforming is a signal processing technique extensively utilized in wireless communications and radars for desired signal intensification and interference signal minimization through spatial selectivity. In this paper, we present a method for calculation of optimal weight vectors for smart antenna array, to achieve a directive pattern during transmission and selective reception in interference prone environment. In proposed scheme, Mutual Information (MI) extrema are evaluated through an energy constrained objective function, which is based on a-priori information of interference source and desired array factor. Signal to Interference plus Noise Ratio (SINR) performance is evaluated for both transmission and reception. In our scheme, MI is presented as an index to identify trade-off between information gain, SINR, illumination time and spatial selectivity in an energy constrained optimization problem. The employed method yields lesser computational complexity, which is presented through comparative analysis with conventional methods in vogue. MI based beamforming offers enhancement of signal integrity in degraded environment while reducing computational intricacy and correlating key performance indicators.

Keywords: beamforming, interference, mutual information, wireless communications

Procedia PDF Downloads 260

Authors: Arias M. L., D’Adamo J., Novosad M. N., Raffo P. A., Burbridge H. P., Artana G.

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Shale oils are highly paraffinic and, consequently, can create wax deposits that foul pipelines during transportation. Several factors must be considered when designing pipelines or treatment programs that prevents wax deposition: including chemical species in crude oils, flowrates, pipes diameters and temperature. This paper describes the wax deposition study carried out within the framework of Y-TEC's flow assurance projects, as part of the process to achieve a better understanding on wax deposition issues. Laboratory experiments were performed on a medium size, 1 inch diameter, wax deposition loop of 15 mts long equipped with a solid detector system, online microscope to visualize crystals, temperature and pressure sensors along the loop pipe. A baseline test was performed with diesel with no paraffin or additive content. Tests were undertaken with different temperatures of circulating and cooling fluid at different flow conditions. Then, a solution formed with a paraffin added to the diesel was considered. Tests varying flowrate and cooling rate were again run. Viscosity, density, WAT (Wax Appearance Temperature) with DSC (Differential Scanning Calorimetry), pour point and cold finger measurements were carried out to determine physical properties of the working fluids. The results obtained in the loop were analyzed through momentum balance and heat transfer models. To determine possible paraffin deposition scenarios temperature and pressure loop output signals were studied. They were compared with WAT static laboratory methods. Finally, we scrutinized the effect of adding a chemical inhibitor to the working fluid on the dynamics of the process of wax deposition in the loop.

Keywords: paraffin desposition, flow assurance, chemical inhibitors, flow loop

Procedia PDF Downloads 83

Authors: Madhu Gupta, G. P. Agrawa, Suresh P. Vyas

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Certain tumor cells overexpress a membrane-spanning molecule aminopeptidase N (CD13) isoform, which is the receptor for peptides containing the NGR motif. NGR-modified Docetaxel (DTX)-loaded PEG-b-PLGA polymeric nanoparticles (cNGR-DNB-NPs) were developed and evaluated for their in vitro potential in HT-1080 cell line. The cNGR-DNB-NPs containing particles were about 148 nm in diameter with spherical shape and high encapsulation efficiency. Cellular uptake was confirmed both qualitatively and quantitatively by Confocal Laser Scanning Microscopy (CLSM) and flow cytometry. Both quantitatively and qualitatively results confirmed the NGR conjugated nanoparticles revealed the higher uptake of nanoparticles by CD13-overexpressed tumor cells. Free NGR inhibited the cellular uptake of cNGR-DNB-NPs, revealing the mechanism of receptor mediated endocytosis. In vitro cytotoxicity studies demonstrated that cNGR-DNB-NPs, formulation was more cytotoxic than unconjugated one, which were consistent well with the observation of cellular uptake. Hence, the selective delivery of cNGR-DNB-NPs formulation in CD13-overexpressing tumors represents a potential approach for the design of nanocarrier-based dual targeted delivery systems for targeting the tumor cells and vasculature.

Keywords: solid Tumor, docetaxel, targeting, NGR ligand

Procedia PDF Downloads 463

Authors: Hamid Hossein Khezri, Afsaneh Javdani-Mallak

Abstract:

Fast inhibitory neurotransmission in the mammalian nervous system is largely mediated by GABAA receptors, chloride-selective members of the superfamily of pentameric Cys-loop receptors. Cannabidiol (CBD) is one of the members of cannabinoid compounds found in cannabis. CBD and Cannabinol (CBN), as the other extract of plant Cannabis, were able to reduce myofascial pain in rats with immunosuppressive and anti-inflammatory activities. In this study, we accomplished protein-protein BLAST and the sequence was found to be for Gamma-aminobutyric acid receptor subunit alpha-1 (GBRA1) chain A and its 3D structure was subsequently downloaded from Protein Data Bank. The structures of the ligands cannabinol and cannabidiol were obtained from PubChem. After a necessary process of the obtained files, AutoDock Vina was used to performing molecular docking. Docking between the ligands and GBRA1 chain A revealed that cannabinol has a higher affinity to GBRA1 (binding energy = -7.5 kcal/mol) compared to cannabidiol (binding energy = -6.5 kcal/mol). Furthermore, cannabinol seems to be able to interact with 10 residues of the protein, out of which 3 are in the neurotransmitter-gated ion-channel transmembrane domain of GBRA1, whereas cannabidiol interacts with two other residues. Although the results of this project do not indicate the activating /or inhibitory capability of the studied compounds, it suggests that cannabinol can act as a relatively strong ligand for GBRA1.

Keywords: protein-ligand docking, cannabinol, cannabidiol, GBRA1

Procedia PDF Downloads 97

Authors: Yasser Gaber, Mohamed Ismail, Serena Bisagni, Mohamad Takwa, Rajni Hatti-Kaul

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Enzymes are safe and selective catalysts. They skillfully catalyze chemical reactions; however, the native form is not usually suitable for industrial applications. Enzymes are therefore engineered by several techniques to meet the required catalytic task. Clopidogrel is recorded among the five best selling pharmaceutical in 2010 under the brand name Plavix. The commonly used route for production of the drug on an industrial scale is the synthesis of the racemic mixture followed by diastereomeric resolution to obtain the pure S isomer. The process consumes a lot of solvents and chemicals. We have evaluated a biocatalytic cleaner approach for asymmetric hydrolysis of racemic clopidogrel. Initial screening of a selected number of hydrolases showed only one enzyme EST to exhibit activity and selectivity towards the desired stereoisomer. As the crude EST is a mixture of several isoenzymes, a homology model of EST-1 was used in molecular dynamic simulations to study the interaction of the enzyme with R and S isomers of clopidogrel. Analysis of the geometric hindrances of the tetrahedral intermediates revealed a potential site for mutagenesis in order to improve the activity and the selectivity. Single point mutation showed dramatic increase in activity and inversion of the enantioselectivity (400 fold change in E value).

Keywords: biocatalysis, biotechnology, enzyme, protein engineering, molecular modeling

Procedia PDF Downloads 422

Authors: Sakshi Tomar, Renu Chadha

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Cocrystallization comprises a selective route to the intensive design of pharmaceutical products with desired physiochemical and pharmacokinetic properties. The present study is focused on the preparation, characterization, and evaluation of etodolac (ET) co-crystals with coformers nicotinamide (ETNI) and Glutaric acid (ETGA), using cocrystallization approach. Preliminarily examination of the prepared co-crystal was done by differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FT-IR), powder X-ray diffraction (PXRD). DSC thermographs of ETNI and ETGA cocrystals showed single sharp melting endotherms at 144°C and 135°C, respectively, which were different from the melting of drugs and coformers. FT-IR study points towards carbonyl-acid interaction sandwiched between the involving molecules. The emergence of new peaks in the PXRD pattern confirms the formation of new crystalline solid forms. Both the cocrystals exhibited better apparent solubility, and 3.8-5.0 folds increase in IDR were established, as compared to pure etodolac. Evaluations of these solid forms were done using anti-osteoarthritic activities. All the results indicate that etodolac cocrystals possess better anti-osteoarthritic efficacy than free drug. Thus loom of cocrystallization has been found to be a viable approach to resolve the solubility and bioavailability issues that circumvent the use of potential antiosteoarthritic molecules.

Keywords: bioavailability, etodolac, nicotinamide, osteoarthritis

Procedia PDF Downloads 184

Authors: Jungkyun Im

Abstract:

Nonsteroidal anti-inflammatory drugs (NSAIDs) are effective for relieving pain and reducing inflammation. They are nonselective inhibitors of two isoforms of COX, cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2), and thereby inhibiting the production of hormone-like lipid compounds such as, prostaglandins and thromboxanes which cause inflammation, pain, fever, platelet aggregation, etc. In addition, recently there are many research articles reporting the neuroprotective effect of NSAIDs in neurodegenerative diseases, such as Alzheimer’s disease (AD) and Parkinson’s disease (PD). However, the clinical use of NSAIDs in these diseases is limited by low brain distribution. Therefore, in order to assist the in-depth investigation on the pharmaceutical mechanism of flurbiprofen in neuroprotection and to make flurbiprofen a more potent drug to prevent or alleviate neurodegenerative diseases, delivery of flurbiprofen to brain should be effective and sufficient amount of flurbiprofen must penetrate the BBB thus gaining access into the patient’s brain. We have recently developed several types of guanidine-rich molecular carriers with high molecular weights and good water solubility that readily cross the blood-brain barrier (BBB) and display efficient distributions in the mouse brain. The G8 (having eight guanidine groups) molecular carrier based on D-sorbitol was found to be very effective in delivering anticancer drugs to a mouse brain. In the present study, employing the same molecular carrier, we prepared the flurbiprofen conjugate and studied its BBB permeation by mouse tissue distribution study. Flurbiprofen was attached to a molecular carrier with a fluorescein probe and multiple terminal guanidiniums. The conjugate was found to internalize into live cells and readily cross the BBB to enter the mouse brain. Our novel synthetic flurbiprofen conjugate will hopefully delivery NSAIDs into brain, and is therefore applicable to the neurodegenerative diseases treatment or prevention.

Keywords: flurbiprofen, drug delivery, molecular carrier, organic synthesis

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Authors: Atul Kumar, Veeranjaneyulu Gannedi, Qazi Naveed Ahmed

Abstract:

Oligosaccharides, which are essential to all cellular organisms, play vital roles in cell recognition, signaling, and are involved in a broad range of biological processes. The chemical synthesis of carbohydrates represents a powerful tool to provide homogeneous glycans. In carbohydrate synthesis, the major concern is the orthogonal protection of hydroxyl groups that can be unmasked independently. Classical protecting groups include benzyl ethers (Bn), which are normally cleaved through hydrogenolysis or by means of metal reduction, and acetate (Ac), benzoate (Bz) or pivaloate esters, which are removed using base promoted hydrolysis. In present work a series of α-Oxoester (COBz) protected saccharides, with divergent base sensitivity profiles against benzoyl (Bz) and acetyl (Ac), were designed and KHSO₅/CH₃COCl in methanol was identified as an easy, mild, selective and efficient deprotecting reagent for their removal in the perspective of carbohydrate synthesis. Timely monitoring of later reagent was advantageous in establishing both sequential as well as simultaneous deprotecting of COBz, Bz, and Ac. The salient feature of our work is its ease to generate different acceptors using designed monosaccharides. In summary, we demonstrated α-Oxoester (COBz) as a new protecting group for carbohydrates and the application of this group for the synthesis of Glycosylphosphatidylinositol (GPI) anchor are in progress.

Keywords: α-Oxoester, oligosaccharides, new protecting group, acceptor synthesis, glycosylation

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Authors: Farhad Shafiepour Motlagh, Narges Salehi

Abstract:

Purpose: The purpose of this study was to support student strategies for virtual learning in the learning management system. Methodology: The research method was based on grounded theory. The statistical population included all the articles of the ten years 2022-2010, and the sampling method was purposeful to the extent of theoretical saturation (n=31 ). Data collection was done by referring to the authoritative scientific databases of Emerald, Springer, Elsevier, Google Scholar, Sage Publication, and Science Direct. For data analysis, open coding, axial coding, and selective coding were used. Results: The results showed that causal conditions include cognitive empowerment (comprehension, analysis, composition), emotional empowerment (learning motivation, involvement in the learning system, enthusiasm for learning), psychomotor empowerment (learning to master, internalizing learning skills, creativity in learning). Conclusion: Supporting students requires their empowerment in three dimensions: cognitive, emotional empowerment, and psychomotor empowerment. In such a way that by introducing them to enter the learning management system, the capacities of the system, the toolkit of learning in the system, improve the motivation to learn in them, and in such a case, by learning more in the learning management system, they will reach mastery learning.

Keywords: student support, virtual education, learning management system, electronic

Procedia PDF Downloads 279

Authors: Behnam Habibi Dargah

Abstract:

The economics of cost-benefit theory seeks to monitor claims and determine their final price. The cost of litigation is important because it is a measure of the efficiency of the justice system. From an economic point of view, the cost of litigation is considered to be the point of equilibrium of litigation, whereby litigation is regarded as a high-risk investment and is initiated when the costs are less than the probable and expected benefits. Costs are economically separated into private and social costs. Private cost includes material (direct and indirect) and spiritual costs. The social costs of litigation are also subsidized-centric due to the public and governmental nature of litigation and cover both types of bureaucratic bureaucracy and the costs of judicial misconduct. Macroeconomic policy in the economics of justice is the reverse engineering of controlling the social costs of litigation by employing selective litigation and working on the judicial culture to achieve rationality in the monopoly system. Procedures for controlling and managing court costs are also circumscribed to economic patterns in the field. Rational cost allocation model and cost transfer model. The rational allocation model deals with cost-tolerance systems, and the transfer model also considers three models of transferability, including legal, judicial and contractual transferability, which will be described and explored in the present article in a comparative manner.

Keywords: cost of litigation, economics of litigation, private cost, social cost, cost of litigation

Procedia PDF Downloads 106

Authors: Md. Mizanur Rahman, Anquan Liu, Anna Frostegård, Johan Frostegård

Abstract:

The role of the human immune system is essential in cardiovascular diseases and atherosclerosis. Activated cells in atherosclerosis produce abundant amounts of cytokines, but the exact mechanisms involved in the effects of these inflammatory cytokines are not clear in atherosclerosis. In a large clinical cohort, we have previously determined that antibodies against phosphorylcholine (anti-PC) are negatively and independently associated with both development of atherosclerosis and also a low risk of cardiovascular disease. Further, we reported that rheumatoid arthritis patients who were non-responders to TNF-inhibitors, where those with low anti-PC levels. Upon anti-TNF treatment, anti-PC levels increased. We, therefore, hypothesised that proinflammatory cytokines such as TNF could play a role in anti-PC regulation. Peripheral blood mononuclear cells (PBMC) were cultured with or without TNF and anti-TNF. The cell supernatants were collected after six days for ELISA measurements. In separate experiments, cells were cultured for 24 hours in both polystyrene plates and ELISPOT plates under a similar condition for ELISA and ELISPOT assays respectively. Total RNA was extracted after 6 hours of cell culture to perform RT-qPCR. Cell viability was confirmed by trypan blue staining and MTT assays. ELISA measurements detected less than 40% of anti-PC in TNF-treated cells, in comparison to control cells, whereas anti-PC production was recovered by anti-TNF treatment. ELISPOT assays showed that TNF suppresses anti-PC production by inhibiting anti-PC producing B-cells. In addition, RT-qPCR and ELISA showed that TNF also has effects also on B-cell activation as BAFF expression was inhibited by TNF treatment. Atherosclerosis is a major cause of cardiovascular diseases, but anti-PC is a protection marker for atherosclerosis development. Our findings show that TNF is a negative regulator of anti-PC production. Immune modulation and rising of anti-PC could be of major significance for the patients.

Keywords: anti-PC, Anti-TNF, atherosclerosis, cardiovascular diseases, phosphorylecholine

Procedia PDF Downloads 221

Authors: Mohamed H. Khalifa, Fikry I. El-Shahawi, Nabil A. Mansour

Abstract:

The cotton leafworm, Spodoptera littoralis (Boisduval) is a major insect pest of vegetables and cotton crops in Egypt, and exhibits different levels of tolerance to certain insecticides. Chlorantraniliprole has been registered recently in Egypt for control this insect. The susceptibilities of three S. littoralis populations collected from El Behaira governorate, north Egypt to chlorantraniliprole were determined by leaf-dipping technique on 4^th instar larvae. Obvious variation of toxicity was observed among the laboratory susceptible, and three field populations with LC₅₀ values ranged between 1.53 µg/ml and 6.22 µg/ml. However, all the three field populations were less susceptible to chlorantraniliprole than a laboratory susceptible population. The most tolerant populations were sampled from El Delengat (ED) Province where S. littoralis had been frequently challenged by insecticides. Certain enzyme activity assays were carried out to be correlated with the mechanism of the observed field population tolerance. All field populations showed significantly enhanced activities of detoxification enzymes compared with the susceptible strain. The regression analysis between chlorantraniliprole toxicities and enzyme activities revealed that the highest correlation is between α-esterase or β-esterase (α-β-EST) activity and collected field strains susceptibility, otherwise this correlation is not significant (P > 0.05). Synergism assays showed the ED and susceptible strains could be synergized by known detoxification inhibitors such as piperonyl butoxide (PBO), triphenyl phosphate (TPP) and diethyl-maleate (DEM) at different levels (1.01-8.76-fold and 1.09-2.94 fold, respectively), TPP showed the maximum synergism in both strains. The results show that there is a correlation between the enzyme activity and tolerance, and carboxylic-esterase (Car-EST) is likely the main detoxification mechanism responsible for tolerance of S. littoralis to chlorantraniliprole.

Keywords: chlorantraniliprole, detoxification enzymes, Egypt, Spodoptera littoralis

Procedia PDF Downloads 256

Authors: Atefeh Esmailnejad, Gholam Reza Nikbakht Brujeni

Abstract:

The major histocompatibility complex (MHC) is the best-characterized genetic region associated with susceptibility and/or resistance to a wide range of infectious diseases, autoimmune diseases and immune responses to vaccines. It has been demonstrated that there is an association between the MHC and resistance to Marek disease, Newcastle disease, Rous sarcoma tumor, Avian leucosis, Fowl cholera, Salmonellosis and Pasteurellosis in chicken. The present study evaluated the MHC polymorphism and its association with antibody response to Newcastle (ND) vaccine in Iranian native chickens. The MHC polymorphism was investigated using LEI0258 microsatellite locus by PCR-based fragment analysis. LEI0258 microsatellite marker is a genetic indicator for MHC, which is located on microchromosome 16 and strongly associated with serologically defined MHC haplotypes. Antibody titer against ND vaccine was measured by Haemaglutination Inhibition (HI) assay. Statistical analysis was performed using SPSS software (version 21). Total of 13 LEI0258 microsatellite alleles were identified in 72 samples which indicated a high genetic diversity in the population. The association study revealed a significant influence of MHC alleles on immune responses to Newcastle vaccine. 311 and 313 bp alleles were significantly associated with elevated immune responses to Newcastle vaccine (p<0.05). These results would be applicable in designing and improving the populations under selective breeding.

Keywords: chicken, LEI0258, MHC, Newcastle vaccine

Procedia PDF Downloads 412

Authors: A. Alssbaiheen, S. Love

Abstract:

Mobile government (m-government) is one of the promising technologies for developing the governance of developing countries. While developing countries often have less advanced internet infrastructure compared to the developed world, mobile phone penetration is very high in the Gulf Cooperation Council (GCC) countries and mobile internet use offers a means to transcend traditional logistical barriers to accessing government services. The study explores the challenges and opportunities of the mobile government in Saudi Arabia. Semi-structured interviews were conducted with a diverse cohort of Saudi mobile users. A total of 77 semi-structured interviews were collected and subsequently analysed using open, axial, and selective coding. The participants’ responses revealed that many opportunities exist for the development of m-government in Saudi Arabia, including high popular awareness of government initiatives in e-government, and willingness to use such services, largely due to the time-saving and convenience aspects it offers compared with traditional bureaucratic services. However, numerous barriers were identified, including the low quality and speed of the internet, service customization, and concerns about privacy data security. It was also felt that in addition to infrastructure challenges, the traditional bureaucratic attitude of government department would itself hinder the effective deployment and utilization of m-government services.

Keywords: awareness, barriers, challenges, government services, mobile government, m-government, opportunities

Procedia PDF Downloads 449