Search results for: inhibitor designing

Authors: Adira Nofeadri Ryofi, Alvin Andrianus, Anna Khairunnisa, Anugrah Cahyo Widodo, Arbhyando Tri Putrananda, Arsy Imanda N. Raswati, Gita Rahmaningsih, Ina Agustina

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The consumption level of fresh bananas from 2005 until 2010, increased from 8.2 to 10 kg/capita/year. The commercial scale of banana generally harvested when it still green to make the banana avoid physical damage, chemical, and disease after harvest and ripe fruit. That first metabolism activity can be used as a synthesis reaction. Ripening fruit was influenced by ethylene hormone that synthesized in fruit which is experiencing ripe and including hormone in the ripening fruit process in klimaterik phase. This ethylene hormone is affected by the respiration level that would speed up the restructuring of carbohydrates inside the fruit, so the weighting of fruit will be decreased. Compared to other klimaterik fruit, banana is a fruit that has a medium ethylene production rate and the rate of respiration is low. The salicylic acid can regulate the result number of the growth process or the development of fruits and plants. Salicylic acid serves to hinder biosynthesis ethylene and delay senses. The research aims to understand the influence of salicylic acid concentration that derived from the waste of avocado skin in inhibition process to ethylene production that the maturation can be controlled, so it can keep the quality of banana for storage. It is also to increase the potential value of the waste of avocado skin that were still used in industrial cosmetics.

Keywords: ethylene hormone, extract avocado skin, inhibitor, salicylic acid

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Authors: Hatem Ashur Masoud Shreha

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Aromatase inhibitors administered before sexual differentiation of the gonads in chicken embryo can induce sex reversal in female layer chickens (phenotypic male). To analyze the process of sex reversal, we have followed for several months the changes induced by Fadrozole, a nonsteroidal aromatase inhibitor on morphology of female sex-reversed and female sex-reversed supplemented with L-tyrosine which was previously shown to stimulate release of Gn Rh. Fadrozole (1mg/egg) was injected into eggs on day four of incubation before sex differentiation. phenotypic males and phenotypic males treated with L-tyrosine and males hatched from eggs injected Fadrozole were sacrificed by slaughtering at 16 weeks old and the remaining chicks were sacrificed at 28 weeks old. Both sexes from control chickens were sacrificed at the same age (16 &28 weeks). Hatchability, behavior, body weight, shank length, comb weight, testes weight, blood cells count and wattle weight of sex reversal were tested at 16 and 28 weeks. The results showed that body weight, comb weight, wattles weight and shank length of sex-reversed females were significantly different from control female. Behavior of phenotypic males and phenotypic males fed on L-tyrosine showed aggressive sexual behavior like that of control males and absence of laying behavior. In conclusion our results confirm that Fadrazole injection in eggs before sex differentiation produce a male behavior and morphological index of male in female chicken.

Keywords: sex-reversal, fadrozole, phenotypic male, L-tyrosine

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Authors: M. F. Alrubaie, S. A. Salih, W. A. Abbas

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Slurry infiltrated fiber concrete (SIFCON) is considered as a special type of high strength high-performance fiber reinforced concrete, extremely strong, and ductile. The objective of this study is to investigate the durability of SIFCON to corrosion in chloride environments. Six different SIFCON mixes were made in addition to two refinance mixes with 0% and 1.5% steel fiber content. All mixes were exposed to 10% chloride solution for 180 days. Half of the specimens were partially immersed in chloride solution, and the others were exposed to weekly cycles of wetting and drying in 10% chloride solution. The effectiveness of using corrosion inhibitors, mineral admixture, and epoxy protective coating were also evaluated as protective measures to reduce the effect of chloride attack and to improve the corrosion resistance of SIFCON mixes. Corrosion rates, half-cell potential, electrical resistivity, total permeability tests had been monitored monthly. The results indicated a significant improvement in performance for SIFCON mixes exposed to chloride environment, when using corrosion inhibitor or epoxy protective coating, whereas SIFCON mix contained mineral admixture (metakaolin) did not improve the corrosion resistance at the same level. The cyclic wetting and drying exposure were more aggressive to the specimens than the partial immersion in chloride solution although the observed surface corrosion for the later was clearer.

Keywords: chloride attack, chloride environments, corrosion inhibitor, corrosion resistance, durability, SIFCON, slurry infiltrated fiber concrete

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Authors: Gabriel S. De Oliveira, Patricia P. Adriani, Christophe Moriseau, Bruce D. Hammock, Felipe S. Chambergo

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Epoxide hydrolases (EHs) are enzymes that are present in all living organisms and catalyze the hydrolysis of epoxides to the corresponding vicinal diols. EHs have high biotechnological interest for the drug design and chemistry transformation for industries. In this study, we describe the identification of substrates and inhibitors of epoxide hydrolase enzyme from the filamentous fungus Trichoderma reesei (TrEH), and these inhibitors showed the fungal growth inhibitory activity. We have used the cloned enzyme and expressed in E. coli to develop the screening in the library of fluorescent substrates with the objective of finding the best substrate to be used in the identification of good inhibitors for the enzyme TrEH. The substrate (3-phenyloxiranyl)-acetic acid cyano-(6-methoxy-naphthalen-2-yl)-methyl ester showed the highest specific activity and was chosen for the next steps of the study. The inhibitors screening was performed in the library with more than three thousand molecules and we could identify the 6 best inhibitors. The IC50 of these molecules were determined in nM and all the best inhibitors have urea or amide in their structure, because It has been recognized that these groups fit well in the hydrolase catalytic pocket of the epoxide hydrolases. Then the growth of T. reesei in PDA medium containing these TrEH inhibitors was tested, and fungal growth inhibition activity was demonstrated with more than 60% of inhibition of fungus growth in the assay with the TrEH inhibitor with the lowest IC50. Understanding how this EH enzyme from T. reesei responds to inhibitors may contribute for the study of fungal metabolism and drug design against pathogenic fungi.

Keywords: epoxide hydrolases, fungal growth inhibition, inhibitor, Trichoderma reesei

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Authors: Saeid Jalilzadeh

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SVC is one of the most significant devices in FACTS technology which is used in parallel compensation, enhancing the transient stability, limiting the low frequency oscillations and etc. designing a proper controller is effective in operation of svc. In this paper the equations that describe the proposed system have been linearized and then the optimum PID controller has been designed for svc which its optimal coefficients have been earned by chaos algorithm. Quick damping of oscillations of generator is the aim of designing of optimum PID controller for svc whether the input power of generator has been changed suddenly. The system with proposed controller has been simulated for a special disturbance and the dynamic responses of generator have been presented. The simulation results showed that a system composed with proposed controller has suitable operation in fast damping of oscillations of generator.

Keywords: chaos, PID controller, SVC, frequency oscillation

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Authors: Sanjay Singh, Parameswara Rao Vuddanda

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The aim of the present study is study the factual benefit of nano size and surface coating of p-gp efflux inhibitor on enhancement of bioavailability of Berberine chloride (BBR); a p-gp substrate. In addition, 28 days sub acute oral toxicity study was also conducted to assess the toxicity of the formulation on chronic administration. BBR loaded polymeric nanoparticles (BBR-NP) were prepared by nanoprecipitation method. BBR NP were surface coated (BBR-SCNP) with the 1 % w/v of vitamin E TPGS. For bioavailability study, total five groups (n=6) of rat were treated as follows first; pure BBR, second; physical mixture of BBR, carrier and vitamin E TPGS, third; BBR-NP, fourth; BBR-SCNP and fifth; BBR and verapamil (widely used p-gp inhibitor). Blood was withdrawn at pre-set timing points in 24 hrs study and drug was quantified by HPLC method. In oral chronic toxicity study, total four groups (n=6) were treated as follows first (control); water, second; pure BBR, third; BBR surface coated nanoparticles and fourth; placebo BBR surface coated nanoparticles. Biochemical levels of liver (AST, ALP and ALT) and kidney (serum urea and creatinine) along with their histopathological studies were also examined (0-28 days). The AUC of BBR-SCNP was significantly 3.5 folds higher compared to all other groups. The AUC of BBR-NP was 3.23 and 1.52 folds higher compared to BBR solution and BBR with verapamil group, respectively. The physical mixture treated group showed slightly higher AUC than BBR solution treated group but significantly low compared to other groups. It indicates that encapsulation of BBR in nanosize form can circumvent P-gp efflux effect. BBR-NP showed pharmacokinetic parameters (Cmax and AUC) which are near to BBR-SCNP. However, the difference in values of T1/2 and clearance indicate that surface coating with vitamin E TPGS not only avoids the P-gp efflux at its absorption site (intestine) but also at organs which are responsible for metabolism and excretion (kidney and liver). It may be the reason for observed decrease in clearance of BBR-SCNP. No toxicity signs were observed either in biochemical or histopathological examination of liver and kidney during toxicity studies. The results indicate that administration of BBR in surface coated nanoformulation would be beneficial for enhancement of its bioavailability and longer retention in systemic circulation. Further, sub acute oral dose toxicity studies for 28 days such as evaluation of intestine, liver and kidney histopathology and biochemical estimations indicated that BBR-SCNP developed were safe for long use.

Keywords: bioavailability, berberine nanoparticles, p-gp efflux inhibitor, nanoprecipitation method

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Authors: Priyanka Chowdhury, Asitikantha Sarma, Utpal Ghosh

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Hadron therapy using high Linear Energy Transfer (LET) ion beam is producing promising clinical results worldwide. The major advantages are its ability to kill radio-resistant tumor and its anti-metastatic activity. Poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors have been widely used as radiosensitizer, but its role in metastasis is unknown. The purpose of our study was to investigate the effect of PARP-1 depletion in combination with either Carbon Ion Beam (CIB) or gamma irradiation on metastatic potential of cultured cancerous cells. A549 cells were irradiated with CIB (0-4Gy) or gamma (0, 2, 4, 6 and 10 Gy) with and without PARP-1 inhibition. The metastatic potential of the cells was determined by cell migratory assay, expression, and activity of MMP-2 and MMP-9, expression of Cadherin, Fibronectin, and Vimentin. CIB exposure reduced migratory property and activity of MMP-2 and MMP-9 significantly. CIB with PARP-1 inhibition reduced cell migration and Matrix Metalloproteinase (MMPs) activity in a synergistic manner. Expression of MMPs was also down-regulated in CIB and combined treatment. On the contrary, MMP- 2 and MMP-9 activity was significantly increased in gamma irradiated cells but decreased upon combined treatment of gamma and PARP-1 inhibitor. MMPs expression and migration was reduced when gamma irradiation was combined with PARP-1 inhibition. Thus, our study clearly demonstrates that PARP-1 inhibition in combination with either high or low LET can significantly suppress metastatic potential in cancer cells and thereby can be a promising tool in controlling metastatic cancers.

Keywords: high LET, low LET, matrix metalloproteinase (MMP), PARP-1

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Authors: Rohit Sane, Pravin Ghadigaonkar, Purvi Ahuja, Suvarna Tirmare, Archana Kelhe, Kranti Shinde, Rahul Mandole

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To evaluate the efficacy of Comprehensive Diabetic Care Program with the reduction of HbA1c in overweight Diabetes Mellitus Type II patients retrospectively. Methods: Retrospective study was carried out on 34 overweight type II diabetic patients (Mean Age = 54.58 ±11.38 yrs). A total of 34 patients were enrolled after screening of 68 patients (HbA1c 7-10%). The patients were on concomitant drugs namely insulin (11.76%), DPP-4 inhibitor (17.64%), Biguanide (55.88%), Sulfonylurea (52.94%), thiazolidinedione (11.76%), other medications (20.58%) and no allopathic medications (14.70%). The patients were given Comprehensive Diabetic Care Program consisting of panchkarma procedures namely snehana (external oleation), swedana (passive heat therapy) and basti (enema), which was completed in 15 sittings. During the therapy and next 90 days, the patients followed low carbohydrate and moderate protein & fat diet. The primary endpoint of this study was the evaluation of reduction in HbA1c at the end of the follow-up after 90 days. Results: Thirty-four overweight type II diabetic patients (mean age: 54.58[±11.38], HbA1c[7-10%], 67.64% male and 32.35% female) were enrolled in the study. A significant reduction was observed in HbA1c levels (14.30%, p<0.05) at the end of the 90 days follow-up as compared to baseline. Also, BMI was reduced by 5.87%. There was reduction in the usage of the concomitant drugs namely insulin (2.94%), DPP-4 inhibitor (2.94%), Biguanide (32.35%), Sulfonylurea (35.29%), thiazolidinedione (5.88%), other medications(17.64%) and no allopathic medications (32.35%). Conclusion: The results of the study highlight not only in the reduction of HbA1c, but also in BMI and drug tapering of the CDC program in the overweight type II diabetic patients with HbA1c (7-10%).

Keywords: HbA1c, low carb diet, Panchakarma therapy, Type II Diabetes

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Authors: Naveen Kumar, Shyambihari Prajapati

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Industry 4.0 is the fourth industrial revolution that focuses on interconnectivity of machine to machine, human to machine and human to human via Internet of Things (IoT). Technologies of industry 4.0 facilitate communication between human and machine through IoT and forms Cyber-Physical Production System (CPPS). In CPPS, multiple shop floors sensor data are connected through IoT and displayed through sensor dashboard to the operator. These sensor dashboards have enormous amount of information to be presented which becomes complex for operators to perform monitoring, controlling and interpretation tasks. Designing handheld sensor dashboards for supervision task will become a challenge for the interface designers. This paper reports emerging technologies of industry 4.0, changing context of increasing information complexity in consecutive industrial revolutions and upcoming design challenges for interface designers in context of Industry 4.0. Authors conclude that information complexity of sensor dashboards design has increased with consecutive industrial revolutions and designs of sensor dashboard causes cognitive load on users. Designing such complex dashboards interfaces in Industry 4.0 context will become main challenges for the interface designers.

Keywords: Industry4.0, sensor dashboard design, cyber-physical production system, Interface designer

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Authors: Hani M. Alothaid, Louise Robson, Richmond Muimo

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Cystic fibrosis (CF) is a disease that affects respiratory function and in EU it affects about 1 in 2,500 live births with an average 40-year life expectancy. This disease caused by mutations within the gene encoding the CFTR (Cystic Fibrosis Transmembrane Conductance Regulator) chloride channel leading to dysregulation of epithelial fluid transport and chronic lung inflammation, suggesting functional alterations of immune cells. In airways, CFTR been found to form a functional complex with S100A10 and AnxA2 in a cAMP/PKA dependent manner. The multiprotein complex of AnxA2-S100A10 and CFTR is also regulated by calcineurin. The aim of this study was i) to investigate whether chloride ion (Cl−) channels are activated by Pseudomonas aeruginosa lipopolysaccharide (LPS from PA), ii) if this activation is regulated by cAMP/PKA/calcineurin pathway and iii) to investigate the role of LPS-activated Cl− channels in the release of pro-inflammatory cytokines by immune cells. Human peripheral blood monocytes were used in the study. Whole-cell patch records showed that LPS from PA can activate Cl− channels, including CFTR and outwardly-rectifying Cl− channel (ORCC). This activation appears to require an intact PKA/calcineurin signalling pathway. The Gout in the presence of LPS was significantly inhibited by diisothiocyanatostilbene-disulfonic acid (DIDS), an ORCC blocker (p<0.001). The Gout was further suppressed by CFTR(inh)-172, a specific inhibitor for CFTR channels (p<0.001). Monocytes pre-incubated with PKA inhibitor or calcineurin inhibitor before stimulated with LPS from PA that were resulted in DIDS and CFTR(inh)-172 insensitive currents. Activation of both ORCC and CFTR was however, observed in response to monocytes exposure to LPS. Additionally, ELISA showed that the CFTR and ORCC play a role in mediating the release of pro-inflammatory cytokines such as IL-1β upon exposure of monocytes to LPS. However, this secretion was significantly inhibited due to CFTR and ORCC inhibition. However, Cl− may play a role in IL-1β release independent of cAMP/PKA/calcineurin signalling due to the enhancement of IL-1β secretion even when cAMP/PKA/calcineurin pathway was inhibited. In conclusion, our data confirmed that LPS from PA activates Cl− channels in human peripheral blood monocytes. Our data also confirmed that Cl− channels were involved in IL-1β release in monocytes upon exposure to LPS. However, it has been found that PKA and calcineurin does not seem to influence the Cl− dependent cytokine release.

Keywords: cystic fibrosis, CFTR, Annexin A2, S100A10, PP2B, PKA, outwardly-rectifying Cl− channel, Pseudomonas aeruginosa

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

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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

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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

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Authors: Abdul Qader Melhem, Hacene Badache

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This paper deals with the theoretical and experimental study of shear connection via simple steel reinforcement shear connectors, which are steel reinforcing bars bent into L-shapes, instead of commonly used headed studs. This suggested L-shape connectors are readily available construction material in steel reinforcement. The composite section, therefore, consists of steel inverted T-section being embedded within a lightly reinforced concrete flange at the top slab as a unit. It should be noted that the cross section of these composite models involves steel inverted T-beam, replacing the steel top flange of a standard commonly employed I-beam section. The paper concentrates on the elastic and elastic-plastic behavior of these composite models. Failure modes either by cracking of concrete or shear connection be investigated in details. Elastic and elastoplastic formulas of the composite model have been computed for different locations of NA. Deflection formula has been derived, its value was close to the test value. With a supportive designing curve, this curve is valuable for both designing engineers and researchers. Finally, suggested designing curves and valuable equations will be presented. A check is made between theoretical and experimental outcomes.

Keywords: composite, elastic-plastic, failure, inverted T-section, L-Shape connectors

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Authors: Shifu Hu, Qiong Yu, Wei Xia, Changhong Zhu

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Background: P38α MAPK, which is a member of the canonical MAPK family, is activated in response to various extracellular stresses and plays a role in multiple cellular processes. It is well known that p38α MAPK play vital roles in oocyte maturation, but the localization and functional roles of p38α MAPK during the meiotic maturation of rat oocytes remain unknown. Study Design: In this study, western-blot and immunofluorescent staining were used to investigate the expression and subcellular localization of p38α MAPK during the meiotic maturation of rat oocytes. SB203580, a specific inhibitor of p38α MAPK, was used to study the roles of p38α MAPK in the meiotic cell cycle of rat oocytes. Results: The results found that p38α MAPK phosphorylation (p-p38α MAPK, indicative of p38α MAPK activation) was low at the germinal vesicle (GV) stage, increased 3 h after germinal vesicle breakdown (GVBD), and maintained its maximum at MI (metaphase I) or M II (metaphase II). The p-p38α MAPK mainly accumulated in the germinal vesicle and had no obvious expression in the nucleus. From GVBD to M II, p-p38α MAPK was distributed in the cytoplasm around either the chromosomes or the spindle. We used SB203580, an inhibitor of p38α MAPK, to investigate the possible functional role of p38α MAPK during rat oocyte meiotic maturation. Treatment of GV stage oocytes with 20 μM SB203580 blocked p-p38α MAPK activity, and the spindles appeared abnormal. Additionally, the rate of GVBD after 3h of culture with 20 μM SB203580 (58.8%) was significantly inhibited compared with the control (82.5%, p < 0.05), and the polar body extrusion rate after 12 h of culture with SB203580 was also significantly decreased compared with the control (40.1 vs. 73.3%, p < 0.05). Conclusions: These data indicate that p38α MAPK may play a vital role in rat oocyte meiotic maturation.

Keywords: meiotic maturation, oocyte, p38α MAPK, spindle

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Authors: Mona T. Kashef, Omneya M. Helmy

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Multidrug resistant (MDR) bacteria have become a significant public health threat. The prevalence rates, of Gram negative MDR bacteria, are in continuous increase. However, few data are available about these resistant strains. Since, third generation cephalosporins are one of the most commonly used antimicrobials, we set out to investigate the prevalence, different mechanisms and clonal relatedness of multidrug resistance among third generation resistant Gram negative clinical isolates. A total of 114 Gram negative clinical isolates, previously characterized as being resistant to at least one of 3rd generation cephalosporins, were included in this study. Each isolate was tested, using Kirby Bauer disk diffusion method, against its assigned categories of antimicrobials. The role of efflux pump in resistance development was tested by the efflux pump inhibitor-based microplate assay using chloropromazine as an inhibitor. Detecting different aminoglycosides, β-lactams and quinolones resistance genes was done using polymerase chain reaction. The genetic diversity of MDR isolates was investigated using Random Amplification of Polymorphic DNA technique. MDR phenotype was detected in 101 isolates (89%). Efflux pump mediated resistance was detected in 49/101 isolates. Aminoglycosides resistance genes; armA and aac(6)-Ib were detected in one and 53 isolates, respectively. The aac(6)-Ib-cr allele, that also confers resistance to floroquinolones, was detected in 28/53 isolates. β-lactam resistance genes; blaTEM, blaSHV, blaCTX-M group 1 and group 9 were detected in 52, 29, 61 and 35 isolates, respectively. Quinolone resistance genes; qnrA, qnrB and qnrS were detectable in 2, 14, 8 isolates respectively, while qepA was not detectable at all. High diversity was observed among tested MDR isolates. MDR is common among 3rd generation cephalosporins resistant Gram negative bacteria, in Egypt. In most cases, resistance was caused by different mechanisms. Therefore, new treatment strategies should be implemented.

Keywords: gram negative, multidrug resistance, RAPD typing, resistance genes

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Authors: Erina Wulansari, Bambang Soemardiono, Ispurwono Soemarno

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Designing sustainable tourism area is defined as an attempt to design an area, that brings the natural environmental conditions as components are available with a wealth of social conditions and the conservation of natural and cultural heritage. To understanding tourism area in this study is not only focus on the location of the tourist object, but rather to a tourist attraction around the area, tourism objects such as the existence of residential area (settlement), a commercial area, public service area, and the natural environmental area. The principle of success in designing a sustainable tourism area is able to integrate and balance between the limited space and the variety of activities that’s always continuously to growth up. The limited space in this area of tourism needs to be managed properly to minimize the damage of environmental as a result of tourism activities hue. This research aims to identify space in this area of tourism through land suitability approach as an effort to create a sustainable design, especially in terms of ecological. This study will be used several analytical techniques to achieve the research objectives as superimposing analysis with GIS 9.3 software and Analysis Hierarchy Process. Expected outcomes are in the form of classification and criteria of usable space in designing embodiment tourism area. In addition, this study can provide input to the order of settlement patterns as part of the environment in the area of sustainable tourism.

Keywords: sustainable tourism area, land suitability, limited space, environment, criteria

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Authors: Ghasem Yazadani, Hamidreza Ahmadi, Masoud Ahmadi, Sajad Rezazadeh

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In this paper with designing and proposing a compound of a heating and cooling system has been tried to show effect of this system on preventing esophagus cancer that can be caused by hot and cold drinks such as tea, coffee and ice water. This system has been simulated mechanically by fluent software and also has been validated by experimental way and a comprehensive result has been presented. Both of solution ways show that this system can reduce or increase temperature of drink to safe very dramatically and it can be a huge step toward consuming drinks safely and also it can be efficient about time issues. The system consists of a temperature sensor and an electronic controller that has a computer program to act automatically this task. Also this system has been presented after many different simulations and has been tried to find the best one in the point view of velocity of heating and cooling.

Keywords: fluent, heat transfer, controller, esophagus cancer

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Authors: Thapanee Seechaliao

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This research paper presents guiding on how to design social media into higher education courses. The research methodology used a survey approach. The research instrument was a questionnaire about guiding on how to design social media into higher education courses. Thirty-one lecturers completed the questionnaire. The data were scored by frequency and percentage. The research results were the lecturers’ opinions concerning the designing social media into higher education courses as follows: 1) Lecturers deem that the most suitable learning theory is Collaborative Learning. 2) Lecturers consider that the most important learning and innovation Skill in the 21st century is communication and collaboration skills. 3) Lecturers think that the most suitable evaluation technique is authentic assessment. 4) Lecturers consider that the most appropriate portion used as blended learning should be 70% in the classroom setting and 30% online.

Keywords: instructional design, social media, courses, higher education

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Authors: Ahlam Ali, Katrina Lappin, Jaine Blayney, Ken Mills

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Leukaemia is the most frequently (30%) occurring type of paediatric cancer. Of these, approximately 80% are acute lymphoblastic leukaemia (ALL) with acute myeloid leukaemia (AML) cases making up the remaining 20% alongside other leukaemias. Unfortunately, children with AML do not have promising prognosis with only 60% surviving 5 years or longer. It has been highlighted recently the need for age-specific therapies for AML patients, with paediatric AML cases having a different mutational landscape compared with AML diagnosed in adult patients. Drug Repurposing is a recognized strategy in drug discovery and development where an already approved drug is used for diseases other than originally indicated. We aim to identify novel combination therapies with the promise of providing alternative more effective and less toxic induction therapy options. Our in-silico analysis highlighted ‘cell death and survival’ as an aberrant, potentially targetable pathway in paediatric AML patients. On this basis, 83 apoptotic inducing compounds were screened. A preliminary single agent screen was also performed to eliminate potentially toxic chemicals, then drugs were constructed into a pooled library with 10 drugs per well over 160 wells, with 45 possible pairs and 120 triples in each well. Seven cell lines were used during this study to represent the clonality of AML in paediatric patients (Kasumi-1, CMK, CMS, MV11-14, PL21, THP1, MOLM-13). Cytotoxicity was assessed up to 72 hours using CellTox™ Green reagent. Fluorescence readings were normalized to a DMSO control. Z-Score was assigned to each well based on the mean and standard deviation of all the data. Combinations with a Z-Score <2 were eliminated and the remaining wells were taken forward for further analysis. A well was considered ‘successful’ if each drug individually demonstrated a Z-Score <2, while the combination exhibited a Z-Score >2. Each of the ten compounds in one well (155) had minimal or no effect as single agents on cell viability however, a combination of two or more of the compounds resulted in a substantial increase in cell death, therefore the ten compounds were de-convoluted to identify a possible synergistic pair/triple combinations. The screen identified two possible ‘novel’ drug pairing, with BCL2 inhibitor ABT-737, combined with either a CDK inhibitor Purvalanol A, or AKT/ PI3K inhibitor LY294002. (ABT-737- 100 nM+ Purvalanol A- 1 µM) (ABT-737- 100 nM+ LY294002- 2 µM). Three possible triple combinations were identified (LY2409881+Akti-1/2+Purvalanol A, SU9516+Akti-1/2+Purvalanol A, and ABT-737+LY2409881+Purvalanol A), which will be taken forward for examining their efficacy at varying concentrations and dosing schedules, across multiple paediatric AML cell lines for optimisation of maximum synergy. We believe that our combination screening approach has potential for future use with a larger cohort of drugs including FDA approved compounds and patient material.

Keywords: AML, drug repurposing, ABT-737, apoptosis

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Authors: D. Bhowmik, Y. Tian, Q. Yin, F. Zhu

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Cyclic GMP-AMP synthase (cGAS), recognises cytoplasmic double-stranded DNA (dsDNA), indicative of bacterial and viral infections, as well as the leakage of self DNA by cellular dysfunction and stresses, to elicit the host's immune responses. Viruses also have developed numerous strategies to antagonize the cGAS-STING pathway. Kaposi's sarcoma-associated herpesvirus (KSHV) is a human DNA tumor virus that is the causative agent of Kaposi’s sarcoma and several other malignancies. To persist in the host, consequently causing diseases, KSHV must overcome the host innate immune responses, including the cGAS-STING DNA sensing pathway. We already found that ORF52 or KicGAS (KSHV inhibitor of cGAS), an abundant and basic gamma herpesvirus-conserved tegument protein, directly inhibits cGAS enzymatic activity. To better understand the mechanism, we have performed the biochemical and structural characterization of full-length KicGAS and various mutants in regarding binding to DNA. We observed that KicGAS is capable of self-association and identified the critical residues involved in the oligomerization process. We also characterized the DNA-binding of KicGAS and found that KicGAS cooperatively oligomerizes along the length of the double stranded DNA, the highly conserved basic residues at the c-terminal disordered region are crucial for DNA recognition. Deficiency in oligomerization also affects DNA binding. Thus DNA binding by KicGAS sequesters DNA and prevents it from being detected by cGAS, consequently inhibiting cGAS activation. KicGAS homologues also inhibit cGAS efficiently, suggesting inhibition of cGAS is evolutionarily conserved mechanism among gamma herpesvirus. These results highlight the important viral strategy to evade this innate immune sensor.

Keywords: Kaposi's sarcoma-associated herpesvirus, KSHV, cGAS, DNA binding, inhibition

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Authors: A. Monika, Manu Sharma, Hong Boo Lee, Richa Dhingra, Neelima Dhingra

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Nuclear factor-κappa B serve as a molecular lynchpin that links persistent infections and chronic inflammation to increased cancer risk. Inflammation has been recognized as a hallmark and cause of cancer. Natural products present a privileged source of inspiration for chemical probe and drug design. Herbal remedies were the first medicines used by humans due to the many pharmacologically active secondary metabolites produced by plants. Some of the metabolites like Lantadene (pentacyclic triterpenoids) from the weed Lantana camara has been known to inhibit cell division and showed anti-antitumor potential. The C-3 aromatic esters of lantadenes were synthesized, characterized and evaluated for cytotoxicity and inhibitory potential against Tumor necrosis factor alpha-induced activation of Nuclear factor-κappa B in lung cancer cell line A549. The 3-methoxybenzoyloxy substituted lead analogue inhibited kinase activity of the inhibitor of nuclear factor-kappa B kinase in a single-digit micromolar concentration. At the same time, the lead compound showed promising cytotoxicity against A549 lung cancer cells with IC50 ( half maximal inhibitory concentration) of 0.98l µM. Further, molecular docking of 3-methoxybenzoyloxy substituted analogue against Inhibitor of nuclear factor-kappa B kinase (Protein data bank ID: 3QA8) showed hydrogen bonding interaction involving oxygen atom of 3-methoxybenzoyloxy with the Arginine-31 and Glutamine-110. Encouraging results indicate the Lantadene’s potential to be developed as anticancer agents.

Keywords: anticancer, lantadenes, pentacyclic triterpenoids, weed

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Authors: Jayanti De

Abstract:

Users of any urban road infrastructure may be classified into various categories. The current paper intends to see whether the opinions on different environmental and transportation criteria vary significantly among different types of road users or not. The paper addresses this issue by using a unique survey data that has been collected from Kolkata, a highly populated city in India. Multiple criteria should be taken into account while planning on infrastructure development programs. Given limited resources, a welfare maximizing government typically resorts to public opinion by designing surveys for prioritization of one project over another. Designing such surveys can be challenging and costly. Deciding upon whom to include in a survey and how to represent each group of consumers/road-users depend crucially on how opinion for different criteria vary across consumer groups. A unique dataset has been collected from various parts of Kolkata to statistically test (using Kolmogorov-Smirnov test) whether assigning of weights to rank the transportation criteria like congestion, air pollution, noise pollution, and morning/evening delay vary significantly across the various groups of users of such infrastructure. The different consumer/user groups in the dataset include pedestrian, private car owner, para-transit (taxi /auto rickshaw) user, public transport (bus) user and freight transporter among others. Very little evidence has been found that ranking of different criteria among these groups vary significantly. This also supports the hypothesis that road- users/consumers form their opinion by using their long-run rather than immediate experience. As a policy prescription, this implies that under-representation or over-representation of a specific consumer group in a survey may not necessarily distort the overall opinion, since opinions across different consumer groups are highly correlated as evident from this particular case study.

Keywords: multi criteria analysis, project-prioritization, road- users, survey designing

Procedia PDF Downloads 258

Authors: Sahar Shahsavaripour Ghazanfarpour

Abstract:

As our daily life depends on quality of built services by systems and using devices in our environment; so education and model of software′s quality will be so important. By daily growth in software′s systems and using them so much, progressing process and requirements′ evaluation in primary level of progress especially architecture level in software get more important. Modern driver architecture changes an in dependent model of a level into some specific models that their purpose is reducing number of software changes into an executive model. Process of designing software engineering is mid-automated. The needed quality attribute in designing architecture and quality attribute in representation are in architecture models. The main problem is the relationship between needs, and elements in some aspect with implicit models and input sources in process. It’s because there is no detection ability. The MART profile is use to describe real-time properties and perform plat form modeling.

Keywords: MDA, DW, OMG, UML, AKB, software architecture, ontology, evaluation

Procedia PDF Downloads 461

Authors: Sungsoo Na, Chanho Park

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Lung cancer is one of the most common severe diseases driving to the death of a human. Lung cancer can be divided into two cases of small-cell lung cancer (SCLC) and non-SCLC (NSCLC), and about 80% of lung cancers belong to the case of NSCLC. From several studies, the correlation between epidermal growth factor receptor (EGFR) and NSCLCs has been investigated. Therefore, EGFR inhibitor drugs such as gefitinib and erlotinib have been used as lung cancer treatments. However, the treatments result showed low response (10~20%) in clinical trials due to EGFR mutations that cause the drug resistance. Patients with resistance to EGFR inhibitor drugs usually are positive to KRAS mutation. Therefore, assessment of EGFR and KRAS mutation is essential for target therapies of NSCLC patient. In order to overcome the limitation of conventional therapies, overall EGFR and KRAS mutations have to be monitored. In this work, the only detection of EGFR will be presented. A variety of techniques has been presented for the detection of EGFR mutations. The standard detection method of EGFR mutation in ctDNA relies on real-time polymerase chain reaction (PCR). Real-time PCR method provides high sensitive detection performance. However, as the amplification step increases cost effect and complexity increase as well. Other types of technology such as BEAMing, next generation sequencing (NGS), an electrochemical sensor and silicon nanowire field-effect transistor have been presented. However, those technologies have limitations of low sensitivity, high cost and complexity of data analyzation. In this report, we propose a label-free and high-sensitive detection method of lung cancer using quartz crystal microbalance based platform. The proposed platform is able to sense lung cancer mutant DNA with a limit of detection of 1nM.

Keywords: cancer DNA, resonance frequency, quartz crystal microbalance, lung cancer

Procedia PDF Downloads 205

Authors: Winai Mankhatitham

Abstract:

This research investigated groundcover on the roof (green roof) which can reduce the temperature and carbon monoxide. This study is divided into 3 main aspects: 1) Types of groundcover affecting heat reduction, 2) The efficiency on heat reduction of 3 types of groundcover, i.e. lawn, arachis pintoi, and purslane, 3) Database for designing green roof. This study has been designed as an experimental research by simulating the 3 types of groundcover in 3 trays placed in the green house for recording the temperature change for 24 hours. The results showed that the groundcover with the highest heat reduction efficiency was lawn. The dense of the lawn can protect the heat transfer to the soil. For the further study, there should be a comparative study of the thickness and the types of soil to get more information for the suitable types of groundcover and the soil for designing the energy saving green roof.

Keywords: green roof, heat reduction, groundcover, energy saving

Procedia PDF Downloads 491

Authors: Wann-Ming Wey

Abstract:

In recent years, in addition to face the external threats such as energy shortages and climate change, traffic congestion and environmental pollution have become anxious problems for many cities. Considering private automobile-oriented urban development had produced many negative environmental and social impacts, the transit-oriented development (TOD) has been considered as a sustainable urban model. TOD encourages public transport combined with friendly walking and cycling environment designs, however, non-motorized modes help improving human health, energy saving, and reducing carbon emissions. Due to environmental changes often affect the planners’ decision-making; this research applies dynamic network process (DNP) which includes the time dependent concept to promoting friendly walking and cycling environmental designs as an advanced planning support system for environment improvements. This research aims to discuss what kinds of design strategies can improve a friendly walking and cycling environment under TOD. First of all, we collate and analyze environment designing factors by reviewing the relevant literatures as well as divide into three aspects of “safety”, “convenience”, and “amenity” from fifteen environment designing factors. Furthermore, we utilize fuzzy Delphi Technique (FDT) expert questionnaire to filter out the more important designing criteria for the study case. Finally, we utilized DNP expert questionnaire to obtain the weights changes at different time points for each design criterion. Based on the changing trends of each criterion weight, we are able to develop appropriate designing strategies as the reference for planners to allocate resources in a dynamic environment. In order to illustrate the approach we propose in this research, Taipei city as one example has been used as an empirical study, and the results are in depth analyzed to explain the application of our proposed approach.

Keywords: environment planning support systems, walking and cycling, transit-oriented development (TOD), dynamic network process (DNP)

Procedia PDF Downloads 319

Authors: Vishaka Agarwal

Abstract:

Fashion is a dynamic entity. With globalisation, fashion is being retailed out to every corner of the world, and people are becoming fashion aware and adapting to the latest trends and look. In this scenario, the role of fashion in providing social change in society is strong. Every product that we use has a design element in it, and consumers prefer to buy those products. The aim of the paper is to look at the ways in which social change can be brought into society through ethical designing by designers taking into consideration the IPR issues. Review of research done by earlier researchers in studying the work done by designers to achieve social change in the society and also discussions with designers to understand the future plans looking at changing world scenario would be done. The paper concludes that fashion has a dynamic role to play in achieving social change in society, and designers are virtually controlling what people buy, wear, and consume globally. This paper would be useful to the social planners and designers in planning the future of society.

Keywords: fashion designers, ethics, intellectual property right, society

Procedia PDF Downloads 160

Authors: Saeid Jalilzadeh

Abstract:

PID controllers are widely used to control the industrial plants because of their robustness and simple structures. Tuning of the controller's parameters to get a desired response is difficult and time consuming. With the development of computer technology and artificial intelligence in automatic control field, all kinds of parameters tuning methods of PID controller have emerged in endlessly, which bring much energy for the study of PID controller, but many advanced tuning methods behave not so perfect as to be expected. Honey Bee algorithm (HBA) and genetic algorithm (GA) are extensively used for real parameter optimization in diverse fields of study. This paper describes an application of HBA and GA to the problem of designing a PID controller whose parameters comprise proportionality constant, integral constant and derivative constant. Presence of three parameters to optimize makes the task of designing a PID controller more challenging than conventional P, PI, and PD controllers design. The suitability of the proposed approach has been demonstrated through computer simulation using MATLAB/SIMULINK.

Keywords: controller, GA, optimization, PID, PSO

Procedia PDF Downloads 514

Authors: L. Bammou, M. Belkhaouda R. Salghi, L. Bazzi, B. Hammouti

Abstract:

Steel and steel-based alloys of different grades steel are extensively used in numerous applications where acid solutions are widely applied such as industrial acid pickling, industrial acid cleaning and oil-well acidizing. The use of chemical inhibitors is one of the most practical methods for the protection against corrosion in acidic media. Most of the excellent acid inhibitors are organic compounds containing nitrogen, oxygen, phosphorus and sulphur. The use of non-toxic inhibitors called green or eco-friendly environmental inhibitors is one of the solutions possible to prevent the corrosion of the material. These advantages have incited us to draw a large part of program of our laboratory to examine natural substances as corrosion inhibitors such as: prickly pear seed oil, Argan oil, Argan extract, Fennel oil, Rosemary oil, Thymus oil, Lavender oil, Jojoba oil, Pennyroyal Mint oil, and Artemisia. In the present work, we investigate the corrosion inhibition of steel in 1 M HCl by junipers extract using weight loss, potentiodynamic polarization and electrochemical impedance spectroscopy (EIS) methods. The result obtained of junipers extract (JE) shows excellent inhibition properties for the corrosion of C38 steel in 1M HCl at 298K, and the inhibition efficiency increases with increasing of the JE concentration. The inhibitor efficiencies determined by weight loss, Tafel polarisation and EIS methods are in reasonable agreement. Based on the polarisation results, the investigated junipers extract can be classified as mixed inhibitor. The calculated structural parameters show increase of the obtained Rct values and decrease of the capacitance, Cdl, with JE concentration increase. It is suggested to attribute this to the increase of the thickness of the adsorption layer at steel surface. The adsorption model obeys to the Langmuir adsorption isotherm. The adsorption process is a spontaneous and exothermic process.

Keywords: corrosion inhibition, steel, friendly inhibitors, Tafel polarisation

Procedia PDF Downloads 484

Authors: Jatinderkumar R. Saini

Abstract:

E-mail has become a key mechanism of electronic communication. This is truer for professional organizations that like to communicate with their subjects online and are slowly shifting to paper-less office. The current paper focuses specifically on academic institutions offering Engineering course in Gujarat state and attempts for textual analysis of the usernames of the institutional e-mail addresses. We found that the institutions tend to design the username segment of their e-mail addresses by choosing words or combination of words from specific categories. The paper also highlights the use of special characters, digits and random words in designing the usernames. On the sidelines, the paper lists the style of employing department names and designations for the design process. To the best of our knowledge, this is the first formal attempt to analyze the selection of words employed for designing username segment of e-mail addresses of Engineering institutions.

Keywords: e-mail address, institute, engineering, username

Procedia PDF Downloads 304