Search results for: tumor cell lines
Commenced in January 2007
Frequency: Monthly
Edition: International
Paper Count: 4950

Search results for: tumor cell lines

1710 Understanding the Performance and Loss Mechanisms in Ag Alloy CZTS Solar Cells: Photocurrent Generation, Charge Separation, and Carrier Transport

Authors: Kang Jian Xian, Huda Abdullah, Md. Akhtaruzzaman, Iskandar Yahya, Mohd Hafiz Dzarfan Othman, Brian Yulianto

Abstract:

The CZTS absorber layer doped with a silver (Ag) is one of the candidates that suggest improving the efficiency of thin films. Silver element functions to reduce antisite defects, increase grain size and create the plasmonic effect. In this work, an experimental study has been done to investigate the electrical and physical properties of CZTS, ACZTS, and AZTS. Ag replaces the Cu in (Cu1-xAgx)2ZnSnS4 (ACZTS) is up to x ≤1. ACZTS thin-films solar cells have been deposited by sol–the gel spin coating method. There are a total of 19 samples done with 11 significant percentages (0%, 10%, 20%… 100%) to show the whole phenomena of efficiency rate and nine specific percentages to find out the best concentration rate for Ag-doped. The obtained results can be helpful for better understanding ACZTS layers.

Keywords: CZTS, ACZTS, AZTS, silver, antisite, efficiency, thin-film solar cell

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1709 Exploring Factors Related to Unplanning Readmission of Elderly Patients in Taiwan

Authors: Hui-Yen Lee, Hsiu-Yun Wei, Guey-Jen Lin, Pi-Yueh Lee Lee

Abstract:

Background: Unplanned hospital readmissions increase healthcare costs and have been considered a marker of poor healthcare performance. The elderly face a higher risk of unplanned readmission due to elderly-specific characteristics such as deteriorating body functions and the relatively high incidence of complications after treatment of acute diseases. Purpose: The aim of this study was exploring the factors that relate to the unplanned readmission of elderly within 14 days of discharge at our hospital in southern Taiwan. Methods: We retrospectively reviewed the medical records of patients aged ≥65 years who had been re-admitted between January 2018 and December 2018.The Charlson Comorbidity score was calculated using previous used method. Related factors that affected the rate of unplanned readmission within 14 days of discharge were screened and analyzed using the chi-squared test and logistic regression analysis. Results: This study enrolled 829 subjects aged more than 65 years. The numbers of unplanned readmission patients within 14 days were 318 cases, while those did not belong to the unplanned readmission were 511 cases. In 2018, the rate of elderly patients in unplanned 14 days readmissions was 38.4%. The majority patients were females (166 cases, 52.2%), with an average age of 77.6 ± 7.90 years (65-98). The average value of Charlson Comorbidity score was 4.42±2.76. Using logistic regression analysis, we found that the gastric or peptic ulcer (OR=1.917 , P< 0.002), diabetes (OR= 0.722, P< 0.043), hemiplegia (OR= 2.292, P< 0.015), metastatic solid tumor (OR= 2.204, P< 0.025), hypertension (OR= 0.696, P< 0.044), and skin ulcer/cellulitis (OR= 2.747, P< 0.022) have significantly higher risk of 14-day readmissions. Conclusion: The results of the present study may assist the healthcare teams to understand the factors that may affect unplanned readmission in the elderly. We recommend that these teams give efficient approach in their medical practice, provide timely health education for elderly, and integrative healthcare for chronic diseases in order to reduce unplanned readmissions.

Keywords: unplanning readmission, elderly, Charlson comorbidity score, logistic regression analysis

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1708 Anticipating Asthma with Control Environmental Factors and Food

Authors: Destin Kurniawati

Abstract:

Asthma is one of the deadly diseases in the world. According to the World Health Organization in 2012, 300 million people suffer from asthma of different races and classes. An estimated 250,000 people die because of asthma annually.As well as more than 57% of children and 51% of adults with asthma. There two risk factors for asthma. That risk factors are the host and environmental. One of the environmental factors that can bring asthma is allergens. When an allergen enters the body, the allergen binds to IgE and cause cell granulat- issued several mediators such as histamine, leukotrienes, bradykinin or something like that. This will cause localized edema effect on bronchial walls of small, thick mucous secretions in the bronchioles, and bronchial smooth muscle spasm. Then there will be inflammation of the airways. Methodology this research is by literature. Therefore, to anticipate and cope with asthma is to control environmental factors that serve to minimize allergens and controlling one's intake in the form of antioxidant-rich foods. Foods rich in antioxidants serve to improve lung function and decrease symptoms of the disease of the respiratory tract.

Keywords: asthma, deadly disease, allergen, environmental and food control

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1707 Monitoring the Change of Padma River Bank at Faridpur, Bangladesh Using Remote Sensing Approach

Authors: Ilme Faridatul, Bo Wu

Abstract:

Bangladesh is often called as a motherland of rivers. It contains about 700 rivers among all these the Padma River is one of the largest rivers of Bangladesh. The change of river bank and erosion has become a common environmental natural hazard in Bangladesh. The river banks are under intense pressure from natural processes such as erosion and accretion as well as anthropogenic processes such as urban growth and pollution. The Padma River is flowing along ten districts of Bangladesh among all these Faridpur district is most vulnerable to river bank erosion. The severity of the river erosion is so high that each year a thousand of populations become homeless and lose their agricultural lands. Though the Faridpur district is most vulnerable to river bank erosion no specific research has been conducted to identify the changing pattern of river bank along this district. The outcome of the research may serve as guidance to prepare river bank monitoring program and management. This research has utilized integrated techniques of remote sensing and geographic information system to monitor the changes from 1995 to 2015 at Faridpur district. To discriminate the land water interface Modified Normalized Difference Water Index (MNDWI) algorithm is applied and on screen digitization approach is used over MNDWI images of 1995, 2002 and 2015 for river bank line extraction. The extent of changes in the river bank along Faridpur district is estimated through overlaying the digitized maps of all three years. The river bank lines are highlighted to infer the erosion and accretion and the changes are calculated. The result shows that the middle of the river is gaining land through sedimentation and the both side river bank is shifting causing severe erosion that consequently resulting the loss of farmland and homestead. Over the study period from 1995 to 2015 it witnessed huge erosion and accretion that played an active role in the changes of the river bank.

Keywords: river bank, erosion and accretion, change monitoring, remote sensing

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1706 In vitro and in vivo Effects of 'Sonneratia alba' Extract against the Fish Pathogen 'Aphanomyces invadans'

Authors: S. F. Afzali, W. L. Wong

Abstract:

The epizootic ulcerative syndrome (EUS) causes by the oomycete fungus, Aphanomyces invadans; known to be one of the infectious fish diseases for farmed and wild fishes in fresh and brackish-water from the Asia-pacific region, America and Africa. Although, EUS had been documented by the Office International des Epizooties (OIE) since 1995, hitherto, there is neither standard chemical agents that can be used for successful treatment of this destructive infection in the time of outbreak; nor available vaccine for prevention. Plant-based remedies in controlling fish diseases are gaining much attention recently as an alternative to chemical treatments, which possess negative effects to the environment and human. In present study, Sonneratia alba, a mangrove plant belongs to the Sonneratiaceae family, was screened in vitro and in vivo for its antifungal activity against A. invadans mycelium growth and its effects on fish innate immune system and disease resistant. The in vitro tests was performed using the disc diffusion methods with measurements of minimum inhibitory concentration (MIC) and inhibition zone. For in vivo study, the S. alba extract supplemented diets were administrated at 0.0, 1.0%, 3.0%, and 5.0% on healthy goldfish, Carassius auratus, which challenged with A. invadans zoospores (100 spores/ml). To compare the significant differences in the hematological and immunological parameters obtained from the experiments, the data were analysed using the SPSS. The methanol extract of S. alba effectively inhibited the mycelial growth of A. invadans at a minimum concentration of 1000 ppm for agar and filter paper diffusion experiments. In the agar diffusion test, 500 ppm of the extract inhibited the fungus mycelial growth up to 96 hours after exposure. The mycelial growth from the edge of the pre-inoculated A. invadans agar discs treated with S. alba extracts at concentrations of 100, 500 and 1000 ppm were 15, 8 and 0 mm respectively. The results of the filter paper disc test showed that the S. alba extract at its minimal inhibitory concentration (1000 ppm) has similar qualitative inhibitory effect as malachite green at 1 ppm and formalin at 250 ppm. According to the in vivo tests findings, in the infected fish fed with 3.0% and 5.0% supplementation diet, the numbers of white blood cell and myeloperoxidase activity significantly increased after the second week of treatment. Whilst the numbers of red blood cell significantly decreased in the infected fish fed with 0.0 and 1.0% supplementation diet. After the third week of feeding, significant increases in the total protein, albumin level, lysozyme activity were recorded in the infected fish fed with 3.0% and 5.0% supplementation diet. Also, the enriched diets increased the survival rate as compared to the untreated group that suffered from 90% mortality. The present study indicated that S. alba extract may inhibit the mycelial growth of A. invadans effectively, suggesting an alternative to other chemotherapeutic agents, which brought much environmental and health concerns to the public, for EUS treatment.

Keywords: fungal pathogen, goldfish, organic extract, treatment

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1705 Role of Molecular Changes and Immunohistochamical in Early Detection of Colon Cancer

Authors: Fatimah Alhomaid

Abstract:

The present study was planned to investigate the role of molecular changes and immunohistochemical in early detection of colon cancer in Saudi patients. Our results were carried out on 48 patients colon cancer. We obtained our data from laboratory in King Khalid university hospital. The specimens were taken (48) patients with colon cancer 34 male and 14 female and 2 control. The average age of varied from 37-85 years. The tumor was diagnosed as I in tow patients (male and female) and grade 2 in 42 patients (29 male and 13 female) while the grade 3 in 4 patients (all males). The specimens were processed for haematoxylin and eosin staining , immunohistochemical technique and flow cytometry analysis. Our study noted that most patients had adenocarcinoma which characterized by presence of signet-ring cells were very clear in advanced patients of adenocarcinoma. Our sections in adenocarcinoma in grade 2 and stage 3 had an increase in signet ring cells,an increase in the acini of glands and an increase in number of lymphocytes which spread to the muscularis layer. With advancing the disease, there were haemorge in blood and increase in lymphocytes and increase number of nuclei in the tubular glands. Our study was carried on 48 patients, immunohistochemical diagnosis (CK20,PCNA,P53) and the analysis of DNA content by flow cytometry technique. Our study indicated that the presence of correlation between the immunohistochemical analysis for P53 and the grades. The reaction of P53 appeared as strong in nucleus in grades &stage 3 and appeared in other sections as dark brown pigment. Our study indicated that the absence of correlation between the immunohistochemical analysis for pcan and the grades. In our sections, there were strong reactions in the more 80% of nuclei in grade 1& stage 2. Our study indicated that the presence of correlation between the immunohistochemical analysis for CK20 and the grades. Our results indicated the presence of positive reaction in cytoplasm varied from weak to moderate in grade 3 & stage 4. Concerning the Flow cytometry technique our results indicated that the presence of correlation between the DNA and different stages of colon cancer.

Keywords: DNA-CK20, PCNA, P53, colon cancer

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1704 A Comparison of Single Point Incremental Forming Formability between Carbon Steel and Stainless Steel

Authors: Kittiphat Rattanachan

Abstract:

The sheet metal forming process, the raw material mechanical properties are important parameters. This paper is to compare the wall’s incline angle or formability of SS 400 steel and SUS 304 stainless steel in single point incremental forming. The two materials are ferrous base alloy, which have the different cell unit, mechanical property and chemical composition. They were forming into cone shape specimens 100 mm diameter with different wall’s incline angle: 90o, 75o, and 60o. The investigation, the specimens were forming until the surface fracture was occurred. The experimental result showed that both materials with the smaller wall’s incline angle, the higher formability. The formability limited of the ferrous base alloy was approx. 60o wall’s incline angle. By nature, SS 400 was higher formability than SUS 304. This result could be used as the initial utilized data in designing the single point incremental forming parts.

Keywords: NC incremental forming, single point incremental forming, wall incline angle, formability

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1703 Identifying Network Subgraph-Associated Essential Genes in Molecular Networks

Authors: Efendi Zaenudin, Chien-Hung Huang, Ka-Lok Ng

Abstract:

Essential genes play an important role in the survival of an organism. It has been shown that cancer-associated essential genes are genes necessary for cancer cell proliferation, where these genes are potential therapeutic targets. Also, it was demonstrated that mutations of the cancer-associated essential genes give rise to the resistance of immunotherapy for patients with tumors. In the present study, we focus on studying the biological effects of the essential genes from a network perspective. We hypothesize that one can analyze a biological molecular network by decomposing it into both three-node and four-node digraphs (subgraphs). These network subgraphs encode the regulatory interaction information among the network’s genetic elements. In this study, the frequency of occurrence of the subgraph-associated essential genes in a molecular network was quantified by using the statistical parameter, odds ratio. Biological effects of subgraph-associated essential genes are discussed. In summary, the subgraph approach provides a systematic method for analyzing molecular networks and it can capture useful biological information for biomedical research.

Keywords: biological molecular networks, essential genes, graph theory, network subgraphs

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1702 Identification of Conserved Domains and Motifs for GRF Gene Family

Authors: Jafar Ahmadi, Nafiseh Noormohammadi, Sedegeh Fabriki Ourang

Abstract:

GRF, Growth regulating factor, genes encode a novel class of plant-specific transcription factors. The GRF proteins play a role in the regulation of cell numbers in young and growing tissues and may act as transcription activations in growth and development of plants. Identification of GRF genes and their expression are important in plants to performance of the growth and development of various organs. In this study, to better understanding the structural and functional differences of GRFs family, 45 GRF proteins sequences in A. thaliana, Z. mays, O. sativa, B. napus, B. rapa, H. vulgare, and S. bicolor, have been collected and analyzed through bioinformatics data mining. As a result, in secondary structure of GRFs, the number of alpha helices was more than beta sheets and in all of them QLQ domains were completely in the biggest alpha helix. In all GRFs, QLQ, and WRC domains were completely protected except in AtGRF9. These proteins have no trans-membrane domain and due to have nuclear localization signals act in nuclear and they are component of unstable proteins in the test tube.

Keywords: domain, gene family, GRF, motif

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1701 Theoretical and Computational Investigation of PCBM and PC71BM Derivatives using the DFT Method

Authors: Zair Mohammed El Amine, Chemouri Hafida, Derbal Habak Hassina

Abstract:

Organic photovoltaic cells are electronic devices that convert sunlight into electricity. To this end, the number of studies on organic photovoltaic cells (OVCs) is growing, and this trend is expected to continue. Computational studies are still needed to verify and prove the capability of CVOs, specifically the nanometer molecule PCBM, based on successful experimental results. In this paper, we present a theoretical and computational investigation of PCBM and PC71BM derivatives using the DFT method. On this basis, we employ independent and time-dependent density theories. HOMO, LUMO and GAPH-L energies, ionization potentials and electronic affinity are determined and found to be in agreement with experiments. Using DFT theory based on B3LYP and M062X methods with bases 6-31G (d,p) and 6-311G (d), calculations show that the most efficient acceptors are presented in the group of PC71BM derivatives and are in substantial agreement with experiments. The geometries of the structures are optimized by Gaussian 09.

Keywords: PCBM, P3HT, organic cell solar, DFT, TD-DFT

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1700 Key Drivers Influencing the Shopping Behaviour of Customers in Retail Store

Authors: Aamir Hasan, Subhash Mishra

Abstract:

The purpose of the study was to determine the key drivers which influence the shopping behavior of the customers in the retail store. In today‟s competitive world with increasing number of retail stores, the retailers need to be more customer oriented. Retail has changed and expanded in all lines of business, be it apparel,jewelry, footwear, groceries etc. The modern consumer is posing a challenging task for the Indian retailer. More aware, more confident and much more demanding, therefore the retailers are looking for ways to deliver better consumer value and to increase consumer purchase intention. Retailers tend to differentiate themselves by making their service easier to consumers. The study aims to study the key drivers that can influence shopping behavior in retail store. A survey (store intercept) method was employed to elicit primary information from 300 shoppers in different retail stores of Lucknow. The findings reveal the factors that play a greater role in influencing the shopping behavior of customers in retail store. As such, a survey of retail store customers‟ attitude towards reduced price, sales promotion, quality of the products, proximity to the home, customer service, store atmospherics were analyzed to identify the key drivers influencing shopping behavior in retail store. A questionnaire based on a five-item Likert scale, as well as random sampling, was employed for data collection. Data analysis was accomplished using SPSS software. The paper has found shopping experience, store image and value for money as three important variable out of which shopping experience emerged as a dominant factor which influences the consumer's shopping behavior in the retail store. Since the research has established empirical evidences in determining the key drivers which influences the shopping behavior of the customers in the retail store, it serves as a foundation for a deeper probe into the shopping behavior of the customers in the retail store research domain in the Indian context.

Keywords: retail, shopping, customers, questionnaire

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1699 Establishments of an Efficient Platform for Genome Editing in Grapevine

Authors: S. Najafi, E. Bertini, M. Pezzotti, G.B. Tornielli, S. Zenoni

Abstract:

Grapevine is an important agricultural fruit crop plant consumed worldwide and with a key role in the global economy. Grapevine is strongly affected by both biotic and abiotic stresses, which impact grape growth at different stages, such as during plant and berry development and pre- and post-harvest, consequently causing significant economic losses. Recently global warming has propelled the anticipation of the onset of berry ripening, determining the reduction of a grape color and increased volatilization of aroma compounds. Climate change could negatively alter the physiological characteristics of the grape and affect the berry and wine quality. Modern plant breeding can provide tools such as genome editing for improving grape resilience traits while maintaining intact the viticultural and oenological quality characteristics of the genotype. This study aims at developing a platform for genome editing application in grapevine plants with the final goal to improve berry quality, biotic, and abiotic resilience traits. We chose to directly deliver ribonucleoproteins (RNP, preassembled Cas protein and guide RNA) into plant protoplasts, and, from these cell structures, regenerate grapevine plants edited in specific selected genes controlling traits of interest. Edited plants regenerated by somatic embryogenesis from protoplasts will then be sequenced and molecularly characterized. Embryogenic calli of Sultana and Shiraz cultivars were initiated from unopened leaves of in-vitro shoot tip cultures and from stamens, respectively. Leaves were placed on NB2 medium while stamens on callus initiation medium (PIV) medium and incubated in the dark at 28 °C for three months. Viable protoplasts, tested by FDA staining, isolated from embryogenic calli were cultured by disc method at 1*105 protoplasts/ml. Mature well-shaped somatic embryos developed directly in the protoplast culture medium two months later and were transferred in the light into to shooting medium for further growth. Regenerated plants were then transferred to the greenhouse; no phenotypic alterations were observed when compared to non in-vitro cultured plants. The performed experiments allowed to established an efficient protocol of embryogenic calli production, protoplast isolation, and regeneration of the whole plant through somatic embryogenesis in both Sultana and Shiraz. Regenerated plants, through direct somatic embryogenesis deriving from a single cell, avoid the risk of chimerism during the regeneration process, therefore improving the genome editing process. As pre-requisite of genome editing, an efficient method for transfection of protoplast by yellow fluorescent protein (YFP) marker genes was also established and experiments of direct delivery of CRISPR–Cas9 ribonucleoproteins (RNPs) in protoplasts to achieve efficient DNA-free targeted mutations are in progress.

Keywords: CRISPR-cas9, plant regeneration, protoplast isolation, Vitis vinifera

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1698 A Low-Power, Low-Noise and High-Gain 58~66 GHz CMOS Receiver Front-End for Short-Range High-Speed Wireless Communications

Authors: Yo-Sheng Lin, Jen-How Lee, Chien-Chin Wang

Abstract:

A 60-GHz receiver front-end using standard 90-nm CMOS technology is reported. The receiver front-end comprises a wideband low-noise amplifier (LNA), and a double-balanced Gilbert cell mixer with a current-reused RF single-to-differential (STD) converter, an LO Marchand balun and a baseband amplifier. The receiver front-end consumes 34.4 mW and achieves LO-RF isolation of 60.7 dB, LO-IF isolation of 45.3 dB and RF-IF isolation of 41.9 dB at RF of 60 GHz and LO of 59.9 GHz. At IF of 0.1 GHz, the receiver front-end achieves maximum conversion gain (CG) of 26.1 dB at RF of 64 GHz and CG of 25.2 dB at RF of 60 GHz. The corresponding 3-dB bandwidth of RF is 7.3 GHz (58.4 GHz to 65.7 GHz). The measured minimum noise figure was 5.6 dB at 64 GHz, one of the best results ever reported for a 60 GHz CMOS receiver front-end. In addition, the measured input 1-dB compression point and input third-order inter-modulation point are -33.1 dBm and -23.3 dBm, respectively, at 60 GHz. These results demonstrate the proposed receiver front-end architecture is very promising for 60 GHz direct-conversion transceiver applications.

Keywords: CMOS, 60 GHz, direct-conversion transceiver, LNA, down-conversion mixer, marchand balun, current-reused

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1697 Impact of Charging PHEV at Different Penetration Levels on Power System Network

Authors: M. R. Ahmad, I. Musirin, M. M. Othman, N. A. Rahmat

Abstract:

Plug-in Hybrid-Electric Vehicle (PHEV) has gained immense popularity in recent years. PHEV offers numerous advantages compared to the conventional internal-combustion engine (ICE) vehicle. Millions of PHEVs are estimated to be on the road in the USA by 2020. Uncoordinated PHEV charging is believed to cause severe impacts to the power grid; i.e. feeders, lines and transformers overload and voltage drop. Nevertheless, improper PHEV data model used in such studies may cause the findings of their works is in appropriated. Although smart charging is more attractive to researchers in recent years, its implementation is not yet attainable on the street due to its requirement for physical infrastructure readiness and technology advancement. As the first step, it is finest to study the impact of charging PHEV based on real vehicle travel data from National Household Travel Survey (NHTS) and at present charging rate. Due to the lack of charging station on the street at the moment, charging PHEV at home is the best option and has been considered in this work. This paper proposed a technique that comprehensively presents the impact of charging PHEV on power system networks considering huge numbers of PHEV samples with its traveling data pattern. Vehicles Charging Load Profile (VCLP) is developed and implemented in IEEE 30-bus test system that represents a portion of American Electric Power System (Midwestern US). Normalization technique is used to correspond to real time loads at all buses. Results from the study indicated that charging PHEV using opportunity charging will have significant impacts on power system networks, especially whereas bigger battery capacity (kWh) is used as well as for higher penetration level.

Keywords: plug-in hybrid electric vehicle, transportation electrification, impact of charging PHEV, electricity demand profile, load profile

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1696 Microfluidic Method for Measuring Blood Viscosity

Authors: Eunseop Yeom

Abstract:

Many cardiovascular diseases, such as thrombosis and atherosclerosis, can change biochemical molecules in plasma and red blood cell. These alterations lead to excessive increase of blood viscosity contributing to peripheral vascular diseases. In this study, a simple microfluidic-based method is used to measure blood viscosity. Microfluidic device is composed of two parallel side channels and a bridge channel. To estimate blood viscosity, blood samples and reference fluid are separately delivered into each inlet of two parallel side channels using pumps. An interfacial line between blood samples and reference fluid occurs by blocking the outlet of one side-channel. Since width for this interfacial line is determined by pressure ratio between blood and reference flows, blood viscosity can be estimated by measuring width for this interfacial line. This microfluidic-based method can be used for evaluating variations in the viscosity of animal models with cardiovascular diseases under flow conditions.

Keywords: blood viscosity, microfluidic chip, pressure, shear rate

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1695 Ab Initio Study of Structural, Elastic, Electronic and Thermal Properties of Full Heusler

Authors: M. Khalfa, H. Khachai, F. Chiker, K. Bougherara, R. Khenata, G. Murtaza, M. Harmel

Abstract:

A theoretical study of structural, elastic, electronic and thermodynamic properties of Fe2VX, (with X = Al and Ga), were studied by means of the full-relativistic version of the full-potential augmented plane wave plus local orbitals method. For exchange and correlation potential we used both generalized-gradient approximation (GGA) and local-density approximation (LDA). Our calculated ground state properties like as lattice constants, bulk modulus and elastic constants appear more accurate when we employed the GGA rather than the LDA approximation, and these results agree very well with the available experimental and theoretical data. Further, prediction of the thermal effects on some macroscopic properties of Fe2VAl and Fe2VGa are given in this paper using the quasi-harmonic Debye model in which the lattice vibrations are taken into account. We have obtained successfully the variations of the primitive cell volume, volume expansion coefficient, heat capacities and Debye temperature with pressure and temperature in the ranges of 0–40 GPa and 0–1500 K.

Keywords: full Heusler, FP-LAPW, electronic properties, thermal properties

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1694 3D Label-Free Bioimaging of Native Tissue with Selective Plane Illumination Optical Microscopy

Authors: Jing Zhang, Yvonne Reinwald, Nick Poulson, Alicia El Haj, Chung See, Mike Somekh, Melissa Mather

Abstract:

Biomedical imaging of native tissue using light offers the potential to obtain excellent structural and functional information in a non-invasive manner with good temporal resolution. Image contrast can be derived from intrinsic absorption, fluorescence, or scatter, or through the use of extrinsic contrast. A major challenge in applying optical microscopy to in vivo tissue imaging is the effects of light attenuation which limits light penetration depth and achievable imaging resolution. Recently Selective Plane Illumination Microscopy (SPIM) has been used to map the 3D distribution of fluorophores dispersed in biological structures. In this approach, a focused sheet of light is used to illuminate the sample from the side to excite fluorophores within the sample of interest. Images are formed based on detection of fluorescence emission orthogonal to the illumination axis. By scanning the sample along the detection axis and acquiring a stack of images, 3D volumes can be obtained. The combination of rapid image acquisition speeds with the low photon dose to samples optical sectioning provides SPIM is an attractive approach for imaging biological samples in 3D. To date all implementations of SPIM rely on the use of fluorescence reporters be that endogenous or exogenous. This approach has the disadvantage that in the case of exogenous probes the specimens are altered from their native stage rendering them unsuitable for in vivo studies and in general fluorescence emission is weak and transient. Here we present for the first time to our knowledge a label-free implementation of SPIM that has downstream applications in the clinical setting. The experimental set up used in this work incorporates both label-free and fluorescent illumination arms in addition to a high specification camera that can be partitioned for simultaneous imaging of both fluorescent emission and scattered light from intrinsic sources of optical contrast in the sample being studied. This work first involved calibration of the imaging system and validation of the label-free method with well characterised fluorescent microbeads embedded in agarose gel. 3D constructs of mammalian cells cultured in agarose gel with varying cell concentrations were then imaged. A time course study to track cell proliferation in the 3D construct was also carried out and finally a native tissue sample was imaged. For each sample multiple images were obtained by scanning the sample along the axis of detection and 3D maps reconstructed. The results obtained validated label-free SPIM as a viable approach for imaging cells in a 3D gel construct and native tissue. This technique has the potential use in a near-patient environment that can provide results quickly and be implemented in an easy to use manner to provide more information with improved spatial resolution and depth penetration than current approaches.

Keywords: bioimaging, optics, selective plane illumination microscopy, tissue imaging

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1693 Regeneration Study on the Athens City Center: Transformation of the Historical Triangle to “Low Pollution and Restricted Vehicle Traffic Zone”

Authors: Chondrogianni Dimitra, Yorgos J. Stephanedes

Abstract:

The impact of the economic crisis, coupled with the aging of the city's old core, is reflected in central Athens. Public and private users, residents, employees, visitors desire the quality upgrading of abandoned buildings and public spaces through environmental upgrading and sustainable mobility, and promotion of the international metropolitan character of the city. In the study, a strategy for reshaping the character and function of the historic Athenian triangle is proposed, aiming at its economic, environmental, and social sustainable development through feasible, meaningful, and non-landscaping solutions of low cost and high positive impact. Sustainable mobility is the main principle in re-planning the study area and transforming it into a “Low Pollution and Limited Vehicle Traffic Zone” is the main strategy. Τhe proposed measures include the development of pedestrian mobility networks by expanding the pedestrian roads and limited-traffic routes, of bicycle networks based on the approved Metropolitan Bicycle Route of Athens, of public transportation networks with new lines of electric mini-buses, and of new regulations for vehicle mobility in the historic triangle. In addition, complementary actions are proposed regarding the provision of Wi-Fi on fixed track media, development of applications that facilitate combined travel and provide real-time data, integration of micromobility (roller skates, Segway, Hoverboard), and its enhancement as a flexible means of personal mobility, and development of car-sharing, ride-sharing and dynamic carpooling initiatives.

Keywords: regeneration plans, sustainable mobility, environmental upgrading, athens historical triangle

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1692 Detection and Quantification of Viable but Not Culturable Vibrio Parahaemolyticus in Frozen Bivalve Molluscs

Authors: Eleonora Di Salvo, Antonio Panebianco, Graziella Ziino

Abstract:

Background: Vibrio parahaemolyticus is a human pathogen that is widely distributed in marine environments. It is frequently isolated from raw seafood, particularly shellfish. Consumption of raw or undercooked seafood contaminated with V. parahaemolyticus may lead to acute gastroenteritis. Vibrio spp. has excellent resistance to low temperatures so it can be found in frozen products for a long time. Recently, the viable but non-culturable state (VBNC) of bacteria has attracted great attention, and more than 85 species of bacteria have been demonstrated to be capable of entering this state. VBNC cells cannot grow in conventional culture medium but are viable and maintain metabolic activity, which may constitute an unrecognized source of food contamination and infection. Also V. parahaemolyticus could exist in VBNC state under nutrient starvation or low-temperature conditions. Aim: The aim of the present study was to optimize methods and investigate V. parahaemolyticus VBNC cells and their presence in frozen bivalve molluscs, regularly marketed. Materials and Methods: propidium monoazide (PMA) was integrated with real-time polymerase chain reaction (qPCR) targeting the tl gene to detect and quantify V. parahaemolyticus in the VBNC state. PMA-qPCR resulted highly specific to V. parahaemolyticus with a limit of detection (LOD) of 10-1 log CFU/mL in pure bacterial culture. A standard curve for V. parahaemolyticus cell concentrations was established with the correlation coefficient of 0.9999 at the linear range of 1.0 to 8.0 log CFU/mL. A total of 77 samples of frozen bivalve molluscs (35 mussels; 42 clams) were subsequently subjected to the qualitative (on alkaline phosphate buffer solution) and quantitative research of V. parahaemolyticus on thiosulfate-citrate-bile salts-sucrose (TCBS) agar (DIFCO) NaCl 2.5%, and incubation at 30°C for 24-48 hours. Real-time PCR was conducted on homogenate samples, in duplicate, with and without propidium monoazide (PMA) dye, and exposed for 45 min under halogen lights (650 W). Total DNA was extracted from cell suspension in homogenate samples according to bolliture protocol. The Real-time PCR was conducted with species-specific primers for V. parahaemolitycus. The RT-PCR was performed in a final volume of 20 µL, containing 10 µL of SYBR Green Mixture (Applied Biosystems), 2 µL of template DNA, 2 µL of each primer (final concentration 0.6 mM), and H2O 4 µL. The qPCR was carried out on CFX96 TouchTM (Bio-Rad, USA). Results: All samples were negative both to the quantitative and qualitative detection of V. parahaemolyticus by the classical culturing technique. The PMA-qPCR let us individuating VBNC V. parahaemolyticus in the 20,78% of the samples evaluated with a value between the Log 10-1 and Log 10-3 CFU/g. Only clams samples were positive for PMA-qPCR detection. Conclusion: The present research is the first evaluating PMA-qPCR assay for detection of VBNC V. parahaemolyticus in bivalve molluscs samples, and the used method was applicable to the rapid control of marketed bivalve molluscs. We strongly recommend to use of PMA-qPCR in order to identify VBNC forms, undetectable by the classic microbiological methods. A precise knowledge of the V.parahaemolyticus in a VBNC form is fundamental for the correct risk assessment not only in bivalve molluscs but also in other seafood.

Keywords: food safety, frozen bivalve molluscs, PMA dye, Real-time PCR, VBNC state, Vibrio parahaemolyticus

Procedia PDF Downloads 131
1691 Efficient Compact Micro Dielectric Barrier Discharge (DBD) Plasma Reactor for Ozone Generation for Industrial Application in Liquid and Gas Phase Systems

Authors: D. Kuvshinov, A. Siswanto, J. Lozano-Parada, W. Zimmerman

Abstract:

Ozone is well known as a powerful fast reaction rate oxidant. The ozone based processes produce no by-product left as a non-reacted ozone returns back to the original oxygen molecule. Therefore an application of ozone is widely accepted as one of the main directions for a sustainable and clean technologies development. There are number of technologies require ozone to be delivered to specific points of a production network or reactors construction. Due to space constrains, high reactivity and short life time of ozone the use of ozone generators even of a bench top scale is practically limited. This requires development of mini/micro scale ozone generator which can be directly incorporated into production units. Our report presents a feasibility study of a new micro scale rector for ozone generation (MROG). Data on MROG calibration and indigo decomposition at different operation conditions are presented. At selected operation conditions with residence time of 0.25 s the process of ozone generation is not limited by reaction rate and the amount of ozone produced is a function of power applied. It was shown that the MROG is capable to produce ozone at voltage level starting from 3.5kV with ozone concentration of 5.28E-6 (mol/L) at 5kV. This is in line with data presented on numerical investigation for a MROG. It was shown that in compare to a conventional ozone generator, MROG has lower power consumption at low voltages and atmospheric pressure. The MROG construction makes it applicable for emerged and dry systems. With a robust compact design MROG can be used as incorporated unit for production lines of high complexity.

Keywords: dielectric barrier discharge (DBD), micro reactor, ozone, plasma

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1690 Control of Stability for PV and Battery Hybrid System in Partial Shading

Authors: Weiying Wang, Qi Li, Huiwen Deng, Weirong Chen

Abstract:

The abrupt light change and uneven illumination will make the PV system get rid of constant output power, which will affect the efficiency of the grid connected inverter as well as the stability of the system. To solve this problem, this paper presents a strategy to control the stability of photovoltaic power system under the condition of partial shading of PV array, leading to constant power output, improving the capacity of resisting interferences. Firstly, a photovoltaic cell model considering the partial shading is established, and the backtracking search algorithm is used as the maximum power point to track algorithm under complex illumination. Then, the energy storage system based on the constant power control strategy is used to achieve constant power output. Finally, the effectiveness and correctness of the proposed control method are verified by the joint simulation of MATLAB/Simulink and RTLAB simulation platform.

Keywords: backtracking search algorithm, constant power control, hybrid system, partial shading, stability

Procedia PDF Downloads 293
1689 Screening Active Components in YPFS for Regulating Initiative Key Factors in Allergic Inflammation

Authors: Dandan Shen, Hui-zhu Wang, Xi Yu, LiLi Gui, Xiao Wei, Xiao-yan Jiang, Da-wei Wang, Min Hong

Abstract:

Yu-ping-feng-san (YPFS) is a clinical medicine for asthma and other allergic diseases, but the mechanism of YPFS on relapse of allergy is unclear. Currently, people come to realize the epithelial cells(EC) play a key role in stimulating and regulating local immune response. The study of thymic stromal lymphopoietin(TSLP derived from EC provides an important evidence that the EC can regulate immune response to stimulate allergic response. In this study, we observed the effect of YPFS on TSLP in vivo and in vitro. We established a method by using bronchial epithelial cells (16HBE) for screening potential bioactive components by HPLC-MS in YPFS and then analyzed the components in serum containing YPFS by UPLC-MS. The results showed that YPFS could decrease TSLP protein level in OVA-sensitized mice and 16HBE cells. Five components combing with the 16HBE cells were both detected in the serum.

Keywords: TSLP, bronchial epithelial cells, cell-binding, drug-containing serum

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1688 Toxicity of Solenstemma Argel (Hargal ) on Nubian Goats

Authors: Amna B. Medani, M. A. Elbadwi Samia, Hassan A. Khalid

Abstract:

In our study, nine Nubian goat kids were obtained, allotted into three groups, and healthily adapted in pens within the premises of the Veterinary Teaching Hospital, University of Khartoum to be given the oral doses of the dried herb shoots at daily doses of 1 and 5 gm/kg/day with drinking water, while the kids of the control group were left undosed. All goats were slaughtered,if not died, after 35 days. S. argel at the given doses caused signs of arched posture, ruffled hair, shivering and paralysis of limbs. On post mortem, lesions were seen to be hepatic fatty changes, renal necrosis, congested lungs and inflamed intestines. Serum chemistry investigations revealed significant increase (P< 0.05-0.01) in the activities of ALP(alkaline phosphates) and AST( aspartate-aminotransferase) in goats dosed with 5 gm /kg/ day. Also observed were significant increases in inorganic phosphorus and urea concentrations (P < 0.05-0.01) in both dosed goat groups. .Other investigations including the activity of GGT( gamma glutamyltransferase), creatinine, calcium, total protein and albumin illustrated no significant difference from that of the undosed controls. On haematological evaluation , the goat kids dosed with 5 gm/kg/dayshowed a decrease in haemoglobin concentration and red blood cells count of (P < 0.05-0.01).Both groups of dosed goats showed a higher packed cell volume values of (P < 0.05) when compared to the control goats .Mean corpuscular haemoglobin values were not different from those of the control kids. S. argel at the given doses caused signs of arched posture, ruffled hair, shivering and paralysis of limbs. On post mortem, lesions were seen to be hepatic fatty changes, renal necrosis, congested lungs and inflamed intestines. Serum chemistry investigations revealed significant increase (P < 0.05-0.01) in the activities of ALP(alkaline phosphates) and AST( aspartate-aminotransferase) in goats dosed with 5 gm /kg/ day. Also observed were significant increases in inorganic phosphorus and urea concentrations (P < 0.05-0.01) in both dosed goat groups. .Other investigations including the activity of GGT( gamma-glutamyltransferase), creatinine, calcium, total protein and albumin illustrated no significant difference from that of the undosed controls. calcium, total protein and albumin illustrated no significant difference from that of the undosed controls. On haematological evaluation , the goat kids dosed with 5 gm/kg/dayshowed a decrease in haemoglobin concentration and red blood cells count of (P < 0.05-0.01).Both groups of dosed goats showed a higher packed cell volume values of (P < 0.05) when compared to the control goats .Mean corpuscular haemoglobin values were not different from those of the control kids. Data obtained were then discussed to find S. argel irritable to intestines , toxic to the kidney and liver and a haematological mild toxin.Suggestions for future were forwarded.

Keywords: hargal, nubian goats, solenstemma argel, toxicity

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1687 Preoperative versus Postoperative Radiation Therapy in Patients with Soft Tissue Sarcoma of the Extremity

Authors: AliAkbar Hafezi, Jalal Taherian, Jamshid Abedi, Mahsa Elahi, Behnam Kadkhodaei

Abstract:

Background: Soft tissue sarcomas (STS) are generally treated with a combination of limb preservation surgery and radiation therapy. Today, preoperative radiation therapy is considered for accurate treatment volume and smaller field size. Therefore, this study was performed to compare preoperative with postoperative radiation therapy in patients with extremity STS. Methods: In this non-randomized clinical trial, patients with localized extremity STS referred to the orthopedic clinics in Iran from 2021 to 2023 were studied. Patients were randomly divided into two groups: preoperative and postoperative radiation therapy. The two groups of patients were compared in terms of acute (wound dehiscence and infection) and late (limb edema, subcutaneous fibrosis, and joint stiffness) complications and their severity, as well as local recurrence and other one-year outcomes. Results: A total of 80 patients with localized extremity STS were evaluated in two treatment groups. The groups were matched in terms of age, sex, history of diabetes mellitus, hypertension, smoking, involved side, involved extremity, lesion location, and tumor histopathology. The acute complications of treatment in the two groups of patients did not differ significantly (P > 0.05). Of the late complications, only joint stiffness between the two groups had significant statistical differences (P < 0.001). The severity of all three late complications in the postoperative radiation therapy group was significantly higher (P < 0.05). There was no significant difference between the two groups in terms of the rate of local recurrence of other one-year outcomes (P > 0.05). Conclusion: This study showed that in patients with localized extremity STS, the two therapeutic approaches of adjuvant and neoadjuvant radiation therapy did not differ significantly in terms of local recurrence and distant metastasis during the one-year follow-up period and due to fewer late complications in preoperative radiotherapy group, this treatment approach can be a better choice than postoperative radiation therapy.

Keywords: soft tissue sarcoma, extremity, preoperative radiation therapy, postoperative radiation therapy

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1686 Neuroprotective Effect of Chrysin on Thioacetamide-Induced Hepatic Encephalopathy in Rats: Role of Oxidative Stress and TLR-4/NF-κB Pathway

Authors: S. A. El-Marasy, S. A. El Awdan, R. M. Abd-Elsalam

Abstract:

This study aimed to investigate the possible neuroprotective effect of chrysin on thioacetamide (TAA)-induced hepatic encephalopathy in rats. Also, the effect of chrysin on motor impairment, cognitive deficits, oxidative stress, neuroinflammation, apoptosis and histopathological damage was assessed. Male Wistar rats were randomly allocated into five groups. The first group received the vehicle (distilled water) for 21 days and is considered as normal group. While the second one received intraperitoneal dose of TAA (200 mg/kg) at three alternative days during the third week of the experiment to induce HE and is considered as control group. The other three groups were orally administered chrysin for 21 days (25, 50, 100 mg/kg) and starting from day 17; rats received intraperitoneal dose of TAA (200 mg/kg) at three alternative days. Then behavioral, biochemical, histopathological and immunohistochemical analyses were assessed. Then behavioral, biochemical, histopathological and immunohistochemical analyses were assessed. Chrysin reversed TAA-induced motor coordination in rotarod test, cognitive deficits in object recognition test (ORT) and attenuated serum ammonia, hepatic liver enzymes, reduced malondialdehyde (MDA), elevated reduced glutathione (GSH), reduced nuclear factor kappa B (NF-κB), tumor necrosis factor-alpha (TNF-α) and Interleukin-6 (IL-6) brain contents. Chrysin administration also reduced Toll-4 receptor (TLR-4) gene expression, caspase-3 protein expression, hepatic necrosis and astrocyte swelling. This study depicts that chrysin exerted neuroprotective effect in TAA-induced HE rats, evidenced by improvement of cognitive deficits, motor incoordination and histopathological changes such as astrocyte swelling and vacuolization; hallmarks in HE, via reducing hyperammonemia, ameliorating hepatic function, in addition to its anti-oxidant, inactivation of TLR-4/NF-κB inflammatory pathway, and anti-apoptotic effects.

Keywords: chrysin, hepatic encephalopathy, oxidative stress, rats, thioacetamide, TLR4/NF-κB pathway

Procedia PDF Downloads 157
1685 Transcriptome and Metabolome Analysis of a Tomato Solanum Lycopersicum STAYGREEN1 Null Line Generated Using Clustered Regularly Interspaced Short Palindromic Repeats/Cas9 Technology

Authors: Jin Young Kim, Kwon Kyoo Kang

Abstract:

The SGR1 (STAYGREEN1) protein is a critical regulator of plant leaves in chlorophyll degradation and senescence. The functions and mechanisms of tomato SGR1 action are poorly understood and worthy of further investigation. To investigate the function of the SGR1 gene, we generated a SGR1-knockout (KO) null line via clustered regularly interspaced short palindromic repeats (CRISPR)/Cas9-mediated gene editing and conducted RNA sequencing and gas chromatography tandem mass spectrometry (GC-MS/MS) analysis to identify the differentially expressed genes. The SlSGR1 (Solanum lycopersicum SGR1) knockout null line clearly showed a turbid brown color with significantly higher chlorophyll and carotenoid content compared to wild-type (WT) fruit. Differential gene expression analysis revealed 728 differentially expressed genes (DEGs) between WT and sgr1 #1-6 line, including 263 and 465 downregulated and upregulated genes, respectively, for which fold change was >2, and the adjusted p-value was <0.05. Most of the DEGs were related to photosynthesis and chloroplast function. In addition, the pigment, carotenoid changes in sgr1 #1-6 line was accumulated of key primary metabolites such as sucrose and its derivatives (fructose, galactinol, raffinose), glycolytic intermediates (glucose, G6P, Fru6P) and tricarboxylic acid cycle (TCA) intermediates (malate and fumarate). Taken together, the transcriptome and metabolite profiles of SGR1-KO lines presented here provide evidence for the mechanisms underlying the effects of SGR1 and molecular pathways involved in chlorophyll degradation and carotenoid biosynthesis.

Keywords: tomato, CRISPR/Cas9, null line, RNA-sequencing, metabolite profiling

Procedia PDF Downloads 116
1684 Modern Construction Methods and Technologies and Their Impacts on Construction Projects

Authors: Michael Anthony Doherty

Abstract:

Modern Methods of Construction (MMC) is a significant topic in the construction industry; while reviewing (MMC) over different fields that are significant in the modern construction world, the following areas were assessed where (MMC) is developing, supply chain management, automation, digital technology, and new construction technologies. Different methods were considered as an approach to research and exploring areas highlighted within the construction industry that are making advancements using Modern Methods of Construction Methods and Technologies (MCMTs). The research was conducted using the following methodologies, literature review of academic sources, primary and secondary data sources, questionaries, and interviews. The paper is composed of two parts, firstly a literature review and secondly a questionnaire used as the basis for interviews were utilised to achieve the following key objectives: to identify (MCMTs) being implemented in the construction industry, research and compile information with regards to these methods, determine their purpose and their application in the industry, establishing what (MCMTs) are being used in the industry while also determining the success of the methods. The research considers the evolution and development of these methods in projects and within the industry itself. Major findings were as follows; automation technologies such as robotics, offsite fabrication utilising automated production lines are increasingly part of project execution, digital technologies such as AR and VR are increasingly utilised in project co-ordination, (MMCTs) are proving to be a solution to the construction industry problems such as a lack of skilled workforce, hazardous work tasks, and situations, new construction technologies are available and finding their place in mainstream construction, (SCM) and (GSCM) are evolving to new levels using new systems and technologies such as block chain technology as well as Company Size and Project size influence the use of (MMCTs) and the adoption of (MMCTS). In summary the paper endeavours to identify and detail how areas of (MMCTs) are developing and are gaining traction within mainstream construction.

Keywords: automation, digital technology, new construction technologies, supply chain management

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1683 Breeding Cotton for Annual Growth Habit: Remobilizing End-of-season Perennial Reserves for Increased Yield

Authors: Salman Naveed, Nitant Gandhi, Grant Billings, Zachary Jones, B. Todd Campbell, Michael Jones, Sachin Rustgi

Abstract:

Cotton (Gossypium spp.) is the primary source of natural fiber in the U.S. and a major crop in the Southeastern U.S. Despite constant efforts to increase the cotton fiber yield, the yield gain has stagnated. Therefore, we undertook a novel approach to improve the cotton fiber yield by altering its growth habit from perennial to annual. In this effort, we identified genotypes with high-expression alleles of five floral induction and meristem identity genes (FT, SOC1, FUL, LFY, and AP1) from an upland cotton mini-core collection and crossed them in various combinations to develop cotton lines with annual growth habit, optimal flowering time and enhanced productivity. To facilitate the characterization of genotypes with the desired combinations of stacked alleles, we identified markers associated with the gene expression traits via genome-wide association analysis using a 63K SNP Array (Hulse-Kemp et al. 2015 G3 5:1187). Over 14,500 SNPs showed polymorphism and were used for association analysis. A total of 396 markers showed association with expression traits. Out of these 396 markers, 159 mapped to genes, 50 to untranslated regions, and 187 to random genomic regions. Biased genomic distribution of associated markers was observed where more trait-associated markers mapped to the cotton D sub-genome. Many quantitative trait loci coincided at specific genomic regions. This observation has implications as these traits could be bred together. The analysis also allowed the identification of candidate regulators of the expression patterns of these floral induction and meristem identity genes whose functions will be validated via virus-induced gene silencing.

Keywords: cotton, GWAS, QTL, expression traits

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1682 Contraction and Membrane Potential of C2C12 with GTXs

Authors: Bayan Almofty, Yuto Yamaki, Tadamasa Terai, Sadahito Uto

Abstract:

Culture techniques of skeletal muscle cells are advanced in the field of regenerative medicine and applied research of cultured muscle. As applied research of cultured muscle, myopathy (muscles disease) treatment is expected and development bio of actuator is also expected in biomedical engineering. Grayanotoxins (GTXs) is known as neurotoxins that enhance the permeability of cell membrane for Na ions. Grayanotoxins are extracted from a famous Pieris japonica and Ericaceae as well as a phytotoxin. In this study, we investigated the effect of GTXs on muscle cells (C2C12) contraction and membrane potential. Contraction of myotubes is induced by applied external electrical stimulation. Contraction and membrane potential change of skeletal muscle cells are induced by injection of current. We, therefore, concluded that effect of Grayanotoxins on contraction and membrane potential of C2C12 relate to acute toxicity of GTXs.

Keywords: skeletal muscle cells C2C12, grayanotoxins, contraction, membrane potential, acute toxicity, pytotoxin, motubes

Procedia PDF Downloads 501
1681 Synthesis of Quinazoline Derivatives as Selective Inhibitors of Cyclooxygenase-1 Enzyme

Authors: Marcela Dvorakova, Lenka Langhansova, Premysl Landa

Abstract:

A series of quinazoline derivatives bearing aromatic rings in 2- and 4-positions were prepared and tested for their biological activity. Firstly, the compounds were evaluated for their potential to inhibit various kinases, such as autophagy activating kinase ULK1, 3-Phosphoinositide-dependent kinase 1, and TANK-binding kinase 1. None of the compounds displayed any activity on these kinases. Secondly, the compounds were tested for their anti-inflammatory activity expressed as cyclooxygenase (COX) isoforms and 5-lipoxygenase (5-LOX) inhibition. Three of the compounds showed significant selectivity towards COX-1 isoform (COX-2/COX-1 SI = 20-30). They inhibited COX-1 in a single-digit µM range. There was also one compound that exhibited inhibitory activity towards all three tested enzymes in µM range (IC50COX-1 = 1.9 µM; IC50COX-2 and 5-LOX = 10.1µM. COX-1 inhibition was until recently considered undesirable due to COX-1 constitutive expression in most cell types and tissues. Thus, there are not many compounds known with selective COX-1 activity. However, it is now believed that COX-1 plays an important role in the pathophysiology of several acute and chronic disorders, including cancer or neurodegenerative diseases. Thus, the discovery of effective COX-1 selective inhibitors is desirable and important.

Keywords: cyclooxygenases, kinases, lipoxygenases, quinazolines

Procedia PDF Downloads 132