Search results for: competitive binding assay
Commenced in January 2007
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Edition: International
Paper Count: 3117

Search results for: competitive binding assay

2517 Anti-inflammatory and Antioxidant Activity of Heliotropium indicum Linn. Used for Cancer Patients Treatment

Authors: Jitpisute Chunthorng-Orn, Thana Juckmeta, Onmanee Prajuabjinda, Arunporn Itharat

Abstract:

Inflammation and oxidative stress work together to produce symptoms in cancer patients. The whole part of it is used as a preparation to treat cancer patients in Khampramong temple which has been a place of treatment and palliative care for cancer patients since 2005. Thus, the objective of this study was to investigate anti-inflammatory and antioxidant activities of Heliotropium indicum extracts. Dried plant materials were extracted in a similar manner to those practiced by the Khampramong Temple i.e. maceration in 95% ethanol and boiling in water. For anti-inflammation activity, both extracts were tested for suppression of nitric oxide (NO) production in LPS-induced RAW 264.7 cells. They were also tested for antioxidant activity by DPPH radical scavenging assay. This study found that the ethanolic extract of Heliotropium indicum exhibited higher inhibitory activity of NO release than Indomethacin as a positive control (IC50 value of 24.17±2.12 and 34.67±6.23 μg/mL, respectively). For DPPH radical scavenging assay, the ethanolic extract also exhibited antioxidant activity but less than BHT as a antioxidant compound (EC50 values = 28.91±4.26 and 13.08±0.29 μg/mL, respectively). In contrast, its water extract had no inhibitory activity on NO release (IC50 > 100 μg/mL) and no inhibitory activity on DPPH radicals (EC50 values > 100 μg/mL). The results showed correlation between anti-inflammation and antioxidant activity and these results also support using this plant to treat cancer patients.

Keywords: Heliotropium indicum, RAW 264.7, DPPH, Khampramong Temple

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2516 Radioprotective Effects of Selenium and Vitamin-E against 6Mv X-Rays in Human Volunteers Blood Lymphocytes by Micronuclei Assay

Authors: Vahid Changizi, Aram Rostami, Akbar Mosavi

Abstract:

Purpose of study: Critical macromolecules of cells such as DNA are in exposure to damage of free radicals that induced from interaction of ionizing radiation with biological systems. Selenium and vitamin-E are natural compound that has been shown to be a direct free radical scavenger. The aim of this study was to investigate the in vivo/in vitro radioprotective effect of selenium and vitamin-E separately and synergistically against genotoxicity induced by 6MV x-rays irradiation in cultured blood lymphocytes from 15 human volunteers. Methods: Fifteen volunteers were divided in three groups include A, B and C. These groups were given slenium(800 IU), vitamin-E(100 mg) and selenium(400 IU) + vitamin-E(50 mg), respectively. Peripheral blood samples were collected from each group before(0 hr) and 1, 2 and 3 hr after selenium and vitamin-E administration (separately and synergistically). Then the blood samples were irradiated to 200 cGy of 6 Mv x-rays. After that, lymphocyte samples were cultured with mitogenic stimulation to determine the chromosomal aberrations wih micronucleus assay in cytokinesis-blocked binucleated cells. Results: The lymphocytes in the blood samples collected at 1 hr after ingestion selenium and vitamin-E, exposed in vitro to x-rays exhibited a significant decrease in the incidence of micronuclei, compared with control group at 0 hr. The maximum protection and decrease in frequency of micronuclei(50%) was observed at 1 hr after administration of selenium and vitamin-E synergistically. Conclusion: The data suggest that ingestion of selenium and vitamin-E as a radioprotector substances before exposures may reduce genetic damage caused by x-rays irradiation.

Keywords: x-rays, selenium, vitamin-e, lymphocyte, micronuclei

Procedia PDF Downloads 257
2515 A Coevolutionary Framework of Business-IT Alignment through the Lens of Enterprise Architecture

Authors: Mengmeng Zhang, Honghui Chen, Kalle Lyytinen

Abstract:

The major challenges for sustainable business-IT alignment (BITA) in a company root in its volatile external competitive environment, increasingly complex internal relationships, and subversive IT roles. Failure to adequately address BITA results in wasting organizational resources, losing competitive advantages, and failing to produce adequate returns on investments. The coevolution is more suitable to describe the dynamic relationships of business and IT and has received certain attention in recent years. Multiple mechanisms for achieving BITC (e.g., sharing domain knowledge, modular design) were obtained. However, instead of a complete managing process, BITC achievement is still hard to operate in practice. This study emphasizes what the BITC management process looks like and how to execute this coevolution step-by-step. A practical coevolutionary framework that combines the enterprise architecture (EA) method with misalignment analysis is proposed in this paper. It contains steps of EA design, misalignment detection, misalignment correction, and EA management /misalignment prevention. The step of misalignment correction is especially discussed at length. This study also evaluates the proposed framework by comparing the characteristics, principles, and approaches of coevolution in the literature.

Keywords: business-IT alignment, business-IT coevolution, enterprise architecture, misalignment analysis, misalignment correction

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2514 Effects of New Anthraquinone Derivatives on Resistance Ovarian Cancer Cells and The Mechanism Investigation

Authors: Hui-Hsin Huang, Sheng-Tung Huang, Chi-Ming Lee, Chiao-Han Yen, Chun-Mao Lin

Abstract:

At initiation stage, there are no symptoms at initiation stage; however, at late stage, patients suffer symptoms as soon as ovarian cancer metastasis. Moreover, ovarian cancer cells are resistant to some anti-ovarian cancer drugs in clinical. Thus, it is very important to find an effective treatment for resistant ovarian cancer. Anthraquinone derivatives are able to induce DNA damage and lead to cell apoptosis, so several derivatives have been used for clinical application. Therefore, to explore more effective anti-ovarian cancer drugs, this study investigates the mechanism of three new anthraquinone compounds bearing different functional groups to camptothecin-resistance ovarian cell line A2780R2000. Cell viability was determined by MTT assay after treating A2780R2000 with the three new anthraquinone compounds. The results indicated that IC50 values are 33.44μM (Compound I), 25.77μM (Compound II) and 24.59μM (Compound III). Next, through cell cycle analysis, the results demonstrated that three new anthraquinone compounds not only induced A2780R2000 cell cycle arrest at early stage but also apoptosis at late stage. Besides, through apoptosis assay, the results indicated new anthraquinone compound induced apoptosis at late stage. Furthermore, the results of western blot show that the three new anthraquinone compounds lead to A2780R2000 apoptosis through intrinsic pathway. Theses results suggested that three new anthraquinone compounds may be potential new drugs for clinical cancer treatment in the future.

Keywords: anthraquinone, camptothecin, resistance, ovarian cancer

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2513 Antioxidant Properties and Nutritive Value of Raw and Cooked Pool barb (Puntius sophore) of Eastern Himalayas

Authors: Chungkham Sarojnalini, Wahengbam Sarjubala Devi

Abstract:

Antioxidant properties and nutritive values of raw and cooked Pool barb, Puntius sophore (Hamilton-Buchanan) of Eastern Himalayas, India were determined. Antioxidant activity of the methanol extract of the raw, steamed, fried and curried Pool barb was evaluated by using 1,1-diphenyl-2-picrylhydrazyl (DPPH) scavenging assay. In DPPH scavenging assay the IC50 value of the raw, steamed, fried and curried Pool barb was 1.66 microgram/ml, 16.09 microgram/ml, 8.99 microgram/ml, 0.59 microgram/ml whereas the IC50 of the reference ascorbic acid was 46.66 microgram/ml. This results shows that the fish have high antioxidant activity. Protein content was found highest in raw (20.50±0.08%) and lowest in curried (18.66±0.13%). Moisture content in raw, fried and curried was 76.35±0.09, 46.27±0.14 and 57.46±0.24 respectively. Lipid content was recorded 2.46±0.14% in raw and 21.76±0.10% in curried. Ash content varies from 12.57±0.11 to 22.53±0.07%. The total aminoacids were varied from 36.79±0.02 and 288.43±0.12 mg/100 g. Eleven essential mineral elements were found abundant in all the samples. The samples had a considerable amount of Fe ranging from 152.17 to 320.39 milligram/100 gram, Ca 902.06 to 1356.02 milligram/100 gram, Zn 91.07 to 138.14 milligram/100 gram, K 193.25 to 261.56 milligram/100 gram, Mg 225.06 to 229.10 milligram/100 gram. Ni was not detected in the curried fish. The Mg and K contents were significantly decreased in frying method; however the Fe, Cu, Ca, Co and Mn content were increased significantly in all the cooked samples. The Mg and Na contents were significantly increased in curried sample and the Cr content was decreased significantly (p<0.05) in all the cooked samples.

Keywords: antioxidant property, pool barb, minerals, aminoacids, proximate composition, cooking methods

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2512 Phytochemical Screening, Anticancer, Antibacterial and Antioxidant Activities of the Leaf Extracts of Mabolo (Diospyros philippinensis A. DC.)

Authors: Jarel Elgin Tolentino, Arby Denise Nera, Mary Rose Roco, Angela Vianca Aspa, Nikko Beltran, Else Dapat

Abstract:

Drug resistance by cells has been the problem in the medical field for decades now. The use of medicinal plants as a source of creating powerful drugs has been nowadays recognized worldwide to treat such resistant diseases. In the present study, the potential for Diospyros philippinensis A. DC. to inhibit growth of both bacteria and cancer cell line was conducted. The leaf crude extracts were screened for the presence of phytochemicals and examined for potential bioactivities by employing several assays like Kirby-Bauer disc diffusion method, DPPH (2,2-diphenyl-1-picryl-hydrazyl-hydrate) assay and MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) tetrazolium assay for the antibacterial, antioxidant and cytotoxic activities of the extract, respectively. Phytochemical test results of the extracts revealed the presence of alkaloids, flavonoids, saponins, phenols, quinones, cardiac glycosides, phlobatannins, carbohydrate, cardenolides and proteins. The leaf extracts were found to exhibit antibacterial activity against gram-positive bacteria, high antioxidant activity (99.22% ± 0.005) but did not show any sign of cytotoxicity towards HCT116 (ATCC CCL-247). The study therefore concludes that D. philippinensis A. DC. leaf extract can be a source of antibacterial and chemopreventive agents. This claim may be used as basis for future investigation.

Keywords: bioassay, medicinal plants, plant crude extracts, phytochemical screening

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2511 Levels of Selected Adipokines in Women with Gestational Diabetes and Type 2 Diabetes, Their Relationship to Metabolic Parameters

Authors: David Karasek, Veronika Kubickova, Ondrej Krystynik, Dominika Goldmannova, Lubica Cibickova, Jan Schovanek

Abstract:

Introduction: Adiponectin, adipocyte-fatty acid-binding protein (A-FABP), and Wnt1 inducible signaling pathway protein-1 (WISP-1) are adipokines particularly associated with insulin resistance. The aim of the study was to compare their levels in women with gestational diabetes (GDM), type 2 diabetes mellitus (T2DM) and healthy controls and determine their relation with metabolic parameters. Methods: Fifty women with GDM, 50 women with T2DM, and 35 healthy women were included in the study. In addition to adipokines, anthropometric, lipid parameters, and markers, insulin resistance, and glucose control were assessed in all participants. Results: Compared to healthy controls only significantly lower levels of adiponectin were detected in women with GDM, whereas lower levels of adiponectin, higher levels of A-FABP and of WISP-1 were present in women with T2DM. Women with T2DM had also lower levels of adiponectin and higher levels of A-FABP compared to women with GDM. In women with GDM or T2DM adiponectin correlated negatively with body mass index (BMI), triglycerides (TG), C-peptide and positively with HDL-cholesterol; A-FABP positively correlated with BMI, TG, waist, and C-peptide. Moreover, there was a positive correlation between WISP-1 and C-peptide in women with T2DM. Conclusion: Adverse adipokines production detecting dysfunctional fat tissue is in women with GDM less presented than in women with T2DM, but more expressed compared to healthy women. Acknowledgment: Supported by AZV NV18-01-00139 and MH CZ DRO (FNOl, 00098892).

Keywords: adiponectin, adipocyte-fatty acid binding protein, wnt1 inducible signaling pathway protein-1, gestational diabetes, type 2 diabetes mellitus

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2510 Knowledge Diffusion via Automated Organizational Cartography (Autocart)

Authors: Mounir Kehal

Abstract:

The post-globalization epoch has placed businesses everywhere in new and different competitive situations where knowledgeable, effective and efficient behavior has come to provide the competitive and comparative edge. Enterprises have turned to explicit - and even conceptualizing on tacit - knowledge management to elaborate a systematic approach to develop and sustain the intellectual capital needed to succeed. To be able to do that, you have to be able to visualize your organization as consisting of nothing but knowledge and knowledge flows, whilst being presented in a graphical and visual framework, referred to as automated organizational cartography. Hence, creating the ability of further actively classifying existing organizational content evolving from and within data feeds, in an algorithmic manner, potentially giving insightful schemes and dynamics by which organizational know-how is visualized. It is discussed and elaborated on most recent and applicable definitions and classifications of knowledge management, representing a wide range of views from mechanistic (systematic, data driven) to a more socially (psychologically, cognitive/metadata driven) orientated. More elaborate continuum models, for knowledge acquisition and reasoning purposes, are being used for effectively representing the domain of information that an end user may contain in their decision making process for utilization of available organizational intellectual resources (i.e. Autocart). In this paper, we present an empirical research study conducted previously to try and explore knowledge diffusion in a specialist knowledge domain.

Keywords: knowledge management, knowledge maps, knowledge diffusion, organizational cartography

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2509 Novel EGFR Ectodomain Mutations and Resistance to Anti-EGFR and Radiation Therapy in H&N Cancer

Authors: Markus Bredel, Sindhu Nair, Hoa Q. Trummell, Rajani Rajbhandari, Christopher D. Willey, Lewis Z. Shi, Zhuo Zhang, William J. Placzek, James A. Bonner

Abstract:

Purpose: EGFR-targeted monoclonal antibodies (mAbs) provide clinical benefit in some patients with H&N squamous cell carcinoma (HNSCC), but others progress with minimal response. Missense mutations in the EGFR ectodomain (ECD) can be acquired under mAb therapy by mimicking the effect of large deletions on receptor untethering and activation. Little is known about the contribution of EGFR ECD mutations to EGFR activation and anti-EGFR response in HNSCC. Methods: We selected patient-derived HNSCC cells (UM-SCC-1) for resistance to mAb Cetuximab (CTX) by repeated, stepwise exposure to mimic what may occur clinically and identified two concurrent EGFR ECD mutations (UM-SCC-1R). We examined the competence of the mutants to bind EGF ligand or CTX. We assessed the potential impact of the mutations through visual analysis of space-filling models of the native sidechains in the original structures vs. their respective side-chain mutations. We performed CRISPR in combination with site-directed mutagenesis to test for the effect of the mutants on ligand-independent EGFR activation and sorting. We determined the effects on receptor internalization, endocytosis, downstream signaling, and radiation sensitivity. Results: UM-SCC-1R cells carried two non-synonymous missense mutations (G33S and N56K) mapping to domain I in or near the EGF binding pocket of the EGFR ECD. Structural modeling predicted that these mutants restrict the adoption of a tethered, inactive EGFR conformation while not permitting association of EGFR with the EGF ligand or CTX. Binding studies confirmed that the mutant, untethered receptor displayed a reduced affinity for both EGF and CTX but demonstrated sustained activation and presence at the cell surface with diminished internalization and sorting for endosomal degradation. Single and double-mutant models demonstrated that the G33S mutant is dominant over the N56K mutant in its effect on EGFR activation and EGF binding. CTX-resistant UM-SCC-1R cells demonstrated cross-resistance to mAb Panitumuab but, paradoxically, remained sensitive to the reversible receptor tyrosine kinase inhibitor Erlotinib. Conclusions: HNSCC cells can select for EGFR ECD mutations under EGFR mAb exposure that converge to trap the receptor in an open, constitutively activated state. These mutants impede the receptor’s competence to bind mAbs and EGF ligand and alter its endosomal trafficking, possibly explaining certain cases of clinical mAb and radiation resistance.

Keywords: head and neck cancer, EGFR mutation, resistance, cetuximab

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2508 Inhibitory Effect of Lactic Acid Bacteria on Uropathogenic Escherichia coli-Induced Urinary Tract Infections

Authors: Cheng-Chih Tsai, Yu-Hsuan Liu, Cheng-Ying Ho, Chun-Chin Huang

Abstract:

The aim of this study evaluated the in vitro and in vivo antimicrobial activity of selected lactic acid bacteria (LAB) against Uropathogenic Escherichia coli (UPEC) for prevention and amelioration of UTIs. We screened LAB strains with antimicrobial effects on UPEC using a well-diffusion assay, bacterial adherence to the uroepithelium cell line SV-HUC-1 (BCRC 60358), and a coculture inhibition assay. The results showed that the 7 LAB strains (Lactobacillus paracasei, L. salivarius, two Pediococcus pentosaceus strains, two L. plantarum strains, and L. crispatus) and the fermented probiotic products produced by these multi-LAB strains exhibited potent zones of inhibition against UPEC. Moreover, the LAB strains and probiotic products adhered strongly to the uroepithelium SV-HUC-1 cell line. The growth of UPEC strains was also markedly inhibited after co-culture with the LAB strains and probiotic products in human urine. In addition, the enhanced levels of IL-6, IL-8 and lactic acid dehydrogenase were significantly decreased by treatments with the LAB strains and probiotic products in UPEC-induced SV-HUC-1 cells. Furthermore, oral administration of probiotic products reduced the number of viable UPEC in the urine of UPEC-challenged BALB/c mice. Taken together, this study demonstrates that probiotic supplementation may be useful as an adjuvant therapy for the treatment of bacterial-induced urinary tract infections.

Keywords: lactic acid bacterium, SV-HUC-1 uroepithelium, urinary tract infection, uropathogenic Escherichia coli, BALB/c mice

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2507 Importance of Positive Education: A Focus on the Importance of Character Strength Building

Authors: Hajra Hussain

Abstract:

Positive education, the inclusion of social, emotional and intellectual skills across a curriculum, is fundamental to the optimal functioning of young people in any society because it combines the best teaching practices with the principles of positive psychology. While learning institutions foster academic skills, little attention is being paid to the identification and development of character strengths and their integration into teaching. There is an increasing recognition of the important role education plays in equipping today’s youth with 21st century social skills. For youth to succeed in this highly competitive environment, there is a need for positive education that is focused on character strengths such as the growth of social, emotional and intellectual skills that promote the flourishing of well-rounded individuals. Character strength programs and awareness are a necessity if the human capital within a region is to be competitive, productive and happy. The Counselling & Wellbeing Centre at Amity University Dubai has consistently implemented Character Strength awareness workshops and has found that such workshops have increased student life satisfaction due to individual awareness of signature strengths. A positive education/positive psychology framework with its key focus on the development of character strengths can be fundamental to individual's confidence and self-awareness; thus allowing both optimum flourishing and functioning.

Keywords: positive psychology, positive education, strengths, youth, happiness

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2506 A Structure-Switching Electrochemical Aptasensor for Rapid, Reagentless and Single-Step, Nanomolar Detection of C-Reactive Protein

Authors: William L. Whitehouse, Louisa H. Y. Lo, Andrew B. Kinghorn, Simon C. C. Shiu, Julian. A. Tanner

Abstract:

C-reactive protein (CRP) is an acute-phase reactant and sensitive indicator for sepsis and other life-threatening pathologies, including systemic inflammatory response syndrome (SIRS). Currently, clinical turn-around times for established CRP detection methods take between 30 minutes to hours or even days from centralized laboratories. Here, we report the development of an electrochemical biosensor using redox probe-tagged DNA aptamers functionalized onto cheap, commercially available screen-printed electrodes. Binding-induced conformational switching of the CRP-targeting aptamer induces a specific and selective signal-ON event, which enables single-step and reagentless detection of CRP in as little as 1 minute. The aptasensor dynamic range spans 5-1000nM (R=0.97) or 5-500nM (R=0.99) in 50% diluted human serum, with a LOD of 3nM, corresponding to 2-orders of magnitude sensitivity under the clinically relevant cut-off for CRP. The sensor is stable for up to one week and can be reused numerous times, as judged from repeated real-time dosing and dose-response assays. By decoupling binding events from the signal induction mechanism, structure-switching electrochemical aptamer-based sensors (SS-EABs) provide considerable advantages over their adsorption-based counterparts. Our work expands on the retinue of such sensors reported in the literature and is the first instance of an SS-EAB for reagentless CRP detection. We hope this study can inspire further investigations into the suitability of SS-EABs for diagnostics, which will aid translational R&D toward fully realized devices aimed at point-of-care applications or for use more broadly by the public.

Keywords: structure-switching, C-reactive protein, electrochemical, biosensor, aptasensor.

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2505 Implementing Online Applications to Allow Marketing Personnel to Share Their Experiences

Authors: Ishak Kamal Baskhayroun

Abstract:

This study examines consumer attitudes toward mobile marketing, especially toward SMS marketing. Unlike similar studies, this study does not focus on the young, but includes consumers who are in the 18-70 age range to the field research. According to the results, it has been concluded that most participants think SMS marketing is disturbing. Most important problems with SMS marketing are about getting subscribed to message lists without the permission of the receiver; the high number of messages sent; and the irrelevancy of the message content. The emergence of sponsorship as a new marketing communication tool and a source of competitive advantage in the marketplace has changed the entire marketing communication process. Sponsorship has overtaken other marketing communication tools in terms of growth and expenditure. This paper seeks to evaluate the role of sponsorship in marketing communication tools. The study recommends that proper measures be taken before the company embarks into sponsorship programs. This is necessary because investment in sponsorship does not always guarantee sustainable competitive advantage in the marketplace.Mobile phones are one of the direct marketing tools that can be used to reach today’s hard to reach consumers. Mobile phones are very personal devices and they are always carried with the consumer, where ever they go. This creates an opportunity for marketers to create personalized marketing communications messages and send them on the right time and place.

Keywords: employee organizational performance, internal marketing, internal customer, direct marketing, mobile phones mobile marketing, sms advertising, marketing sponsorship, marketing communication theories, marketing communication tools corporate responsibility

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2504 Organizational Management and Leadership

Authors: Osman Yildiz

Abstract:

As it is predicted 2559 years before there is nothing permanent except change. In our turbulent World, Organizations will always be faced with the challenge of determining the path that will always keep them on balance en route that will bring success. That means from top to bottom, every organisation is exposed to fight to stay afloat and compete while they face the continuous prospect of change in an increasingly competitive and globalized World. Otherwise, they would fail to realize their goals and targets, and ultimately would disappear. But the organizations that will celebrate success five or ten years from now will be the winners of the fight by having recognizing that planning the change was only the first step in the journey and put sufficient efforts into the task of leading change. Increasingly unpredictable and competitive organizational environments have put pressure on leaders across all industries to better manage the change. The key of establishing effective change and transformation in organisations lies on the steps taken before the change happens depending to the quality of the human sources; readiness for change, acknowledgement by management, prepared leaders, motivated employees, overcoming the resistance to change and ultimately adapting change into the organization. Due to these factors, leaders managing the organisational development can ensure organizations and employees to meet new performance targets, motivation and skills rapidly and effectively. Finally, this article will provide some tools for leaders, and discuss how to catch organisational development and manage the innovations in effective ways.

Keywords: managing the change, organizational change, human factor, leaders, globalization, organisational development

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2503 Partial Replacement for Cement and Coarse Aggregate in Concrete by Using Egg Shell Powder and Coconut Shell

Authors: A. K. Jain, M. C. Paliwal

Abstract:

The production of cement leads to the emission of large amounts of carbon-dioxide gas into the atmosphere which is a major contributor for the greenhouse effect and the global warming; hence it is mandatory either to quest for another material or partly replace it with some other material. According to the practical demonstrations and reports, Egg Shell Powder (ESP) can be used as a binding material for different field applications as it contains some of the properties of lime. It can partially replace the cement and further; it can be used in different proportion for enhancing the performance of cement. It can be used as a first-class alternative, for material reuse and waste recycling practices. Eggshell is calcium rich and analogous to limestone in chemical composition. Therefore, use of eggshell waste for partial replacement of cement in concrete is feasible. Different studies reveal that plasticity index of the soil can be improved by adding eggshell wastes in all the clay soil and it has wider application in construction projects including earth canals and earthen dams. The scarcity of aggregates is also increasing nowadays. Utilization of industrial waste or secondary materials is increasing in different construction applications. Coconut shell was successfully used in the construction industry for partial or full replacement for coarse aggregates. The use of coconut shell gives advantage of using waste material to partially replace the coarse aggregate. Studies carried on coconut shell indicate that it can partially replace the aggregate. It has good strength and modulus properties along with the advantage of high lignin content. It absorbs relatively low moisture due to its low cellulose content. In the paper, study carried out on eggshell powder and coconut shell will be discussed. Optimum proportions of these materials to be used for partial replacement of cement and aggregate will also be discussed.

Keywords: greenhouse, egg shell powder, binding material, aggregates, coconut shell, coarse aggregates

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2502 The Influence of Amygdalin on Glioblastoma Multiforme Cell Lines

Authors: Sylwia K. Naliwajko, Justyna Moskwa, Patryk Nowakowski, Renata Markiewicz-Zukowska, Krystyna Gromkowska-Kepka, Anna Puscion-Jakubik, Maria H. Borawska

Abstract:

Amygdalin is found in many fruit seeds, including apricot, peach, quince, apples, and almonds. Amygdalin (also named vitamin B17), as well as its sources, are commonly used as an alternative therapy or prevention of cancer. The potential activity of amygdalin is related to its enzymatic degradation to the hydrogen cyanide. Hydrogen cyanide is a toxic substance that causes liver and nerves damage, fever, coma or even death. Amygdalin is much better tolerated after intravenous than oral administration. The aim of this study was to examine the influence of amygdalin on glioblastoma multiforme cell lines. Three glioblastoma multiforme cell lines – U87MG, T98, LN18 were incubated (48 h) with amygdalin in concentrations 100, 250, 500, 1000 and 2000 µg/mL. The MTT (Thiazolyl Blue Tetrazolium Bromide) test and DNA binding test by [3H]-thymidine incorporation were used to determine the anti-proliferative activity of amygdalin. The secretion of metalloproteinases (MMP2 and MMP-9) from U87MG cells was estimated by gelatin zymography. The statistical analysis was performed using Statistica v. 13.0 software. The data was presented as a % of control. Amygdalin did not show significant inhibition of viability of all the glioblastoma cells in concentrations 100, 250, 500, 1000 µg/mL. In 2000 µg/mL there were significant differences compared to the control, but inhibition of viability was less than 20% (more than 80% of control). The average viability of U87MG cells was 92,0±4%, T98G: 85,8±3% and LN18: 94,7±2% of the control. There was no dose-response viability, and IC50 value was not recognized. DNA binding in U87MG cells was not inhibited (109,0±3 % of control). After treatment with amygdalin, we observed significantly increased secretion of MMP2 and MMP9 in U87MG cells (130,3±14% and 112,0±5% of control, respectively). Our results suggest that amygdalin has no anticancer activity in glioblastoma cell lines.

Keywords: amygdalin, anticancer, cell line, glioblastoma

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2501 Effects of Opuntia ficus-indica var. Saboten on Glucose Uptake and Insulin Sensitivity in Pancreatic β Cell

Authors: Kang-Hyun Leem, Myung-Gyou Kim, Hye Kyung Kim

Abstract:

The prickly pear cactus (Opuntia ficus-indica) has a global distribution and have been used for medicinal benefits such as artherosclerosis, diabetes, gastritis, and hyperglycemia. However, very little information is currently available for their mechanism. The prikly pear variety Opuntia ficus-indica var. Saboten (OFS) is widely cultivated in Cheju Island, southwestern region of Korea, and used as a functional food. Present study investigated the effects of OFS on pancreatic β-cell function using pancreatic islet β cells (HIT cell). Alpha-glucosidase inhibition, glucose uptake, insulin secretion, insulin sensitivity, and pancreatic β cell proliferation were determined. The inhibitory effect of ethanol extract of OFS stem on α-glucosidase enzyme was measured in a cell free system. Glucose uptake was determined using fluorescent glucose analogue, 2-NBDG. Insulin secretion was measured by ELISA assay. Cell proliferation was measured by MTT assay. Ethanol extracts of OFS dose-dependently inhibited α-glucosidase activity as well as glucose uptake. Insulinotrophic effect of OFS extract was observed at high glucose media in pancreatic β-islet cells. Furthermore, pancreatic β cell regeneration was also observed.These results suggest that OFS mediates the antidiabetic activity mainly via α-glucosidase inhibition, glucose uptake, and improved insulin sensitivity.

Keywords: prickly pear cactus, Opuntia ficus-indica var. Saboten, pancreatic islet HIT cells, α-glucosidase, glucose uptake, insulinotrophic

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2500 In Vitro Antioxidant and Cytotoxic Activities Against Human Oral Cancer and Human Laryngeal Cancer of Limonia acidissima L. Bark Extracts

Authors: Kriyapa lairungruang, Arunporn Itharat

Abstract:

Limonia acidissima L. (LA) (Common name: wood apple, Thai name: ma-khwit) is a medicinal plant which has long been used in Thai traditional medicine. Its bark is used for treatment of diarrhea, abscess, wound healing and inflammation and it is also used in oral cancer. Thus, this research aimed to investigate antioxidant and cytotoxic activities of the LA bark extracts produced by various extraction methods. Different extraction procedures were used to extract LA bark for biological activity testing: boiling in water, maceration with 95% ethanol, maceration with 50% ethanol and water boiling of each the 95% and the 50% ethanolic residues. All extracts were tested for antioxidant activity using DPPH radical scavenging assay, cytotoxic activity against human laryngeal epidermoid carcinoma (HEp-2) cells and human oral epidermoid carcinoma (KB) cells using sulforhodamine B (SRB) assay. The results found that the 95% ethanolic extract of LA bark showed the highest antioxidant activity with EC50 values of 29.76±1.88 µg/ml. For cytotoxic activity, the 50% ethanolic extract showed the best cytotoxic activity against HEp-2 and KB cells with IC50 values of 9.55±1.68 and 18.90±0.86 µg/ml, respectively. This study demonstrated that the 95% ethanolic extract of LA bark showed moderate antioxidant activity and the 50% ethanolic extract provided potent cytotoxic activity against HEp-2 and KB cells. These results confirm the traditional use of LA for the treatment of oral cancer and laryngeal cancer, and also support its ongoing use.

Keywords: antioxidant activity, cytotoxic activity, Laryngeal epidermoid carcinoma, Limonia acidissima L., oral epidermoid carcinoma

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2499 Knowledge Diffusion via Automated Organizational Cartography: Autocart

Authors: Mounir Kehal, Adel Al Araifi

Abstract:

The post-globalisation epoch has placed businesses everywhere in new and different competitive situations where knowledgeable, effective and efficient behaviour has come to provide the competitive and comparative edge. Enterprises have turned to explicit- and even conceptualising on tacit- Knowledge Management to elaborate a systematic approach to develop and sustain the Intellectual Capital needed to succeed. To be able to do that, you have to be able to visualize your organization as consisting of nothing but knowledge and knowledge flows, whilst being presented in a graphical and visual framework, referred to as automated organizational cartography. Hence, creating the ability of further actively classifying existing organizational content evolving from and within data feeds, in an algorithmic manner, potentially giving insightful schemes and dynamics by which organizational know-how is visualised. It is discussed and elaborated on most recent and applicable definitions and classifications of knowledge management, representing a wide range of views from mechanistic (systematic, data driven) to a more socially (psychologically, cognitive/metadata driven) orientated. More elaborate continuum models, for knowledge acquisition and reasoning purposes, are being used for effectively representing the domain of information that an end user may contain in their decision making process for utilization of available organizational intellectual resources (i.e. Autocart). In this paper we present likewise an empirical research study conducted previously to try and explore knowledge diffusion in a specialist knowledge domain.

Keywords: knowledge management, knowledge maps, knowledge diffusion, organizational cartography

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2498 Deciphering Specific Host-Selective Toxin Interaction of Cassiicolin with Lipid Membranes and its Cytotoxicity on Rubber Leaves

Authors: Kien Xuan Ngo

Abstract:

Cassiicolin (Cas), a toxin produced by Corynespora cassiicola, is responsible for corynespora leaf fall (CLF) disease in rubber trees. Currently, the molecular mechanism of the cytotoxicity of Cas isoforms (i.e., Cas1, Cas2) on rubber leaves and its host selectivity have not been fully elucidated. This study analyzed the binding of Cas1 and Cas2 to membranes consisting of different plant lipids and their membrane-disruption activities. Using high-speed atomic force microscopy and confocal microscopy, this study reveals that the binding and disruption activities of Cas1 and Cas2 on lipid membranes are strongly dependent on the specific plant lipids. The negative phospholipids, glycerolipids, and sterols are more susceptible to membrane damage caused by Cas1 and Cas2 than neutral phospholipids and betaine lipids. In summary, This study unveils that (i) Cas1 and Cas2 directly damage and cause necrosis in the leaves of specific rubber clones; (ii) Cas1 and Cas2 can form biofilm-like structures on specific lipid membranes (negative phospholipids, glycerolipids, and sterols). The biofilm-like formation of Cas toxin plays an important role in selective disruption on lipid membranes; (iii) Vulnerability of the specific cytoplasmic membranes to the selective Cas toxin is the most remarkable feature of cytotoxicity of Cas toxin on plant cells. Finally, researcher’s exploration is crucial to understand the basic molecular mechanism underlying the host-selective toxic interaction of Cas toxin with cytoplasmic membranes in plant cells.

Keywords: cassiicolin, corynespora leaf fall disease, high-speed AFM, giant liposome vesicles

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2497 Chemical Analysis, Antioxidant Activity and Antimicrobial Activity of Isolated Compounds and Essential Oil from Callistemon citrinus Leaf

Authors: Manal M. Hamed, Mosad A. Ghareeb, Abdel-Aleem H. Abdel-Aleem, Amal M. Saad, Mohamed S. Abdel-Aziz, Asmaa H. Hadad

Abstract:

Natural products derived from medicinal plants provide unlimited opportunities for a new medication leads because of the unmatched accessibility of chemical variation. Six compounds were isolated from the n-butanol extract of Callistemon citrinus (Family Myrtaceae), they were identified as; nepetolide (1), callislignan A (2), 6,8-dimethoxy-4,5-dimethyl-3-methyleneisochroman-1-one (3), 3-methyl-7-O-benzoyl-β-D-glucopyranoside (4), 5, 7, 3', 5'-tetrahydroxy-6, 8-di-C-methyl flavanone (5), and (2R,3R,4S,5S)-2,4-bis(4-hydroxyphenyl)-3,5-dihydroxy-tetrahydropyran (6). The isolated compounds were evaluated as antioxidant and antimicrobial agents. The antioxidant activities of the compounds were determined using DPPH-radical scavenging and total antioxidant capacity (TAC) assays. The results indicated that compound (5) was most active in its capacity to scavenge free radicals in the DPPH assay [SC50 value, 4.65 ± 0.74μg/mL] compared to the standard ascorbic acid and exhibited the highest activity in the TAC assay (610.45 ± 1.67mg AAE/g compound). The pure isolates were tested for their antimicrobial activity against four pathogenic microbial strains including Staphylococcus aureus, Methicillin-resistant Staphylococcus aureus (MRSA), Pseudomonas aeruginosa and Candida albicans. Also, the GC/MS analysis of its leaves essential oil presented nine identified compounds representing 91% of the total oil constituents. The outcomes got from this study give a reasonable justification for the medicinal uses of Callistemon citrinus plant.

Keywords: Callistemon citrinus, flavanone, antioxidant activity, antimicrobial activity, essential oil, Myrtaceae

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2496 Antifungal Activity of Medicinal Plants Used Traditionally for the Treatment of Fungal Infections and Related Ailments in South Africa

Authors: T. C. Machaba, S. M. Mahlo

Abstract:

The current study investigates the antifungal properties of crude plant extracts from selected medicinal plant species. Eight plant species used by the traditional healers and local people to treat fungal infections were selected for further phytochemical analysis and biological assay. The selected plant species were extracted with solvent of various polarities such as acetone, methanol, ethanol, hexane, dichloromethane, ethyl acetate and water. Leaf, roots and bark extracts of Maerua juncea Pax, Albuca seineri (Engl & K. Krause) J.C Manning & Goldblatt, Senna italica Mill., Elephantorrhiza elephantina (Burch.) Skeels, Indigofera circinata Benth., Schinus molle L., Asparagus buchananii Bak., were screened for antifungal activity against three animal fungal pathogens (Candida albicans, Aspergillus fumigatus and Cryptococcus neoformans). All plant extracts were active against the tested microorganisms. Acetone, dichloromethane, hexane and ethanol extracts of Senna italica and Elephantorrhiza elephantine had excellent activity against Candida albicans and A. fumigatus with the lowest MIC value of 0.02 mg/ml. Bioautography assay was used to determine the number of antifungal compounds presence in the plant extracts. No active compounds were observed in plant extracts of Indigofera circinnata, Schinus molle and Pentarrhinum insipidum with good antifungal activity against C. albicans and A. fumigatus indicating possible synergism between separated metabolites.

Keywords: antifungal activity, bioautography, ethnobotanical survey, minimum inhibitory concentration

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2495 Rapid Plasmonic Colorimetric Glucose Biosensor via Biocatalytic Enlargement of Gold Nanostars

Authors: Masauso Moses Phiri

Abstract:

Frequent glucose monitoring is essential to the management of diabetes. Plasmonic enzyme-based glucose biosensors have the advantages of greater specificity, simplicity and rapidity. The aim of this study was to develop a rapid plasmonic colorimetric glucose biosensor based on biocatalytic enlargement of AuNS guided by GOx. Gold nanoparticles of 18 nm in diameter were synthesized using the citrate method. Using these as seeds, a modified seeded method for the synthesis of monodispersed gold nanostars was followed. Both the spherical and star-shaped nanoparticles were characterized using ultra-violet visible spectroscopy, agarose gel electrophoresis, dynamic light scattering, high-resolution transmission electron microscopy and energy-dispersive X-ray spectroscopy. The feasibility of a plasmonic colorimetric assay through growth of AuNS by silver coating in the presence of hydrogen peroxide was investigated by several control and optimization experiments. Conditions for excellent sensing such as the concentration of the detection solution in the presence of 20 µL AuNS, 10 mM of 2-(N-morpholino) ethanesulfonic acid (MES), ammonia and hydrogen peroxide were optimized. Using the optimized conditions, the glucose assay was developed by adding 5mM of GOx to the solution and varying concentrations of glucose to it. Kinetic readings, as well as color changes, were observed. The results showed that the absorbance values of the AuNS were blue shifting and increasing as the concentration of glucose was elevated. Control experiments indicated no growth of AuNS in the absence of GOx, glucose or molecular O₂. Increased glucose concentration led to an enhanced growth of AuNS. The detection of glucose was also done by naked-eye. The color development was near complete in ± 10 minutes. The kinetic readings which were monitored at 450 and 560 nm showed that the assay could discriminate between different concentrations of glucose by ± 50 seconds and near complete at ± 120 seconds. A calibration curve for the qualitative measurement of glucose was derived. The magnitude of wavelength shifts and absorbance values increased concomitantly with glucose concentrations until 90 µg/mL. Beyond that, it leveled off. The lowest amount of glucose that could produce a blue shift in the localized surface plasmon resonance (LSPR) absorption maxima was found to be 10 – 90 µg/mL. The limit of detection was 0.12 µg/mL. This enabled the construction of a direct sensitivity plasmonic colorimetric detection of glucose using AuNS that was rapid, sensitive and cost-effective with naked-eye detection. It has great potential for transfer of technology for point-of-care devices.

Keywords: colorimetric, gold nanostars, glucose, glucose oxidase, plasmonic

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2494 Comparative in silico and in vitro Study of N-(1-Methyl-2-Oxo-2-N-Methyl Anilino-Ethyl) Benzene Sulfonamide and Its Analogues as an Anticancer Agent

Authors: Pamita Awasthi, Kirna, Shilpa Dogra, Manu Vatsal, Ritu Barthwal

Abstract:

Doxorubicin, also known as adriamycin, is an anthracycline class of drug used in cancer chemotherapy. It is used in the treatment of non-Hodgkin’s lymphoma, multiple myeloma, acute leukemias, breast cancer, lung cancer, endometrium cancer and ovary cancers. It functions via intercalating DNA and ultimately killing cancer cells. The major side effects of doxorubicin are hair loss, myelosuppression, nausea & vomiting, oesophagitis, diarrhoea, heart damage and liver dysfunction. The minor modifications in the structure of compound exhibit large variation in the biological activity, has prompted us to carry out the synthesis of sulfonamide derivatives. Sulfonamide is an important feature with broad spectrum of biological activity such as antiviral, antifungal, diuretics, anti-inflammatory, antibacterial and anticancer activities. Structure of the synthesized compound N-(1-methyl-2-oxo-2-N-methyl anilino-ethyl)benzene sulfonamide confirmed by proton nuclear magnetic resonance (1H NMR),13C NMR, Mass and FTIR spectroscopic tools to assure the position of all protons and hence stereochemistry of the molecule. Further we have reported the binding potential of synthesized sulfonamide analogues in comparison to doxorubicin drug using Auto Dock 4.2 software. Computational binding energy (B.E.) and inhibitory constant (Ki) has been evaluated for the synthesized compound in comparison of doxorubicin against Poly (dA-dT).Poly (dA-dT) and Poly (dG-dC).Poly (dG-dC) sequences. The in vitro cytotoxic study against human breast cancer cell lines confirms the better anticancer activity of the synthesized compound over currently in use anticancer drug doxorubicin. The IC50 value of the synthesized compound is 7.12 µM where as for doxorubicin is 7.2 µ.

Keywords: Doxorubicin, auto dock, in silco, in vitro

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2493 Development and Validation of High-Performance Liquid Chromatography Method for the Determination and Pharmacokinetic Study of Linagliptin in Rat Plasma

Authors: Hoda Mahgoub, Abeer Hanafy

Abstract:

Linagliptin (LNG) belongs to dipeptidyl-peptidase-4 (DPP-4) inhibitor class. DPP-4 inhibitors represent a new therapeutic approach for the treatment of type 2 diabetes in adults. The aim of this work was to develop and validate an accurate and reproducible HPLC method for the determination of LNG with high sensitivity in rat plasma. The method involved separation of both LNG and pindolol (internal standard) at ambient temperature on a Zorbax Eclipse XDB C18 column and a mobile phase composed of 75% methanol: 25% formic acid 0.1% pH 4.1 at a flow rate of 1.0 mL.min-1. UV detection was performed at 254nm. The method was validated in compliance with ICH guidelines and found to be linear in the range of 5–1000ng.mL-1. The limit of quantification (LOQ) was found to be 5ng.mL-1 based on 100µL of plasma. The variations for intra- and inter-assay precision were less than 10%, and the accuracy values were ranged between 93.3% and 102.5%. The extraction recovery (R%) was more than 83%. The method involved a single extraction step of a very small plasma volume (100µL). The assay was successfully applied to an in-vivo pharmacokinetic study of LNG in rats that were administered a single oral dose of 10mg.kg-1 LNG. The maximum concentration (Cmax) was found to be 927.5 ± 23.9ng.mL-1. The area under the plasma concentration-time curve (AUC0-72) was 18285.02 ± 605.76h.ng.mL-1. In conclusion, the good accuracy and low LOQ of the bioanalytical HPLC method were suitable for monitoring the full pharmacokinetic profile of LNG in rats. The main advantages of the method were the sensitivity, small sample volume, single-step extraction procedure and the short time of analysis.

Keywords: HPLC, linagliptin, pharmacokinetic study, rat plasma

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2492 The New Insight about Interspecies Transmission of Iranian H9N2 Influenza Viruses from Avian to Human

Authors: Masoud Soltanialvar, Ali Bagherpour

Abstract:

Documented cases of human infection with H9N2 avian influenza viruses, first detected in 1999 in Hong Kong and China, indicate that these viruses can be directly transmitted from birds to humans. In this study, we characterized the mutation in the Hemagglutinin (HA) genes and proteins that correlates with a shift in affinity of the Hemagglutinin (HA) protein from the “avian” type sialic receptors to the “human” type in 10 Iranian isolates. We delineated the genomes and receptor binding profile of HA gene of some field isolates and established their phylogenetic relationship to the other Asian H9N2 sub lineages. A total of 1200 tissue samples collected from 40 farms located in various states of Iran during 2008 – 2010 as part of a program to monitor Avian Influenza Viruses (AIV) infection. To determine the genetic relationship of Iranian viruses, the Hemagglutinin (HA) genes from ten isolates were amplified and sequenced (by RT-PCR method). Nucleotide sequences (orf) of the (HA) genes were used for phylogenetic tree construction. Deduced amino acid sequences showed the presence of L226 (234 in H9 numbering) in all ten Iranian isolates which indicates a preference to binding of α (2–6) sialic acid receptors, so these Iranian H9N2 viruses have the potential to infect human beings. These isolates showed high degree of homology with 2 human H9N2 isolates A/HK/1073/99, A/HK/1074/99. Phylogenetic analysis of showed that all the HA genes of the Iranian H9N2 viruses fall into a single group within a G1-like sublineage which had contributed as donor of six internal genes to H5N1 highly pathogenic avian influenza. The results of this study indicated that all Iranian viruses have the potential to emerge as highly pathogenic influenza virus, and considering the homology of these isolates with human H9N2 strains, it seems that the potential of these avian influenza isolates to infect human should not be overlooked.

Keywords: influenza virus, hemagglutinin, neuraminidase, Iran

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2491 Algorithms Inspired from Human Behavior Applied to Optimization of a Complex Process

Authors: S. Curteanu, F. Leon, M. Gavrilescu, S. A. Floria

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Optimization algorithms inspired from human behavior were applied in this approach, associated with neural networks models. The algorithms belong to human behaviors of learning and cooperation and human competitive behavior classes. For the first class, the main strategies include: random learning, individual learning, and social learning, and the selected algorithms are: simplified human learning optimization (SHLO), social learning optimization (SLO), and teaching-learning based optimization (TLBO). For the second class, the concept of learning is associated with competitiveness, and the selected algorithms are sports-inspired algorithms (with Football Game Algorithm, FGA and Volleyball Premier League, VPL) and Imperialist Competitive Algorithm (ICA). A real process, the synthesis of polyacrylamide-based multicomponent hydrogels, where some parameters are difficult to obtain experimentally, is considered as a case study. Reaction yield and swelling degree are predicted as a function of reaction conditions (acrylamide concentration, initiator concentration, crosslinking agent concentration, temperature, reaction time, and amount of inclusion polymer, which could be starch, poly(vinyl alcohol) or gelatin). The experimental results contain 175 data. Artificial neural networks are obtained in optimal form with biologically inspired algorithm; the optimization being perform at two level: structural and parametric. Feedforward neural networks with one or two hidden layers and no more than 25 neurons in intermediate layers were obtained with values of correlation coefficient in the validation phase over 0.90. The best results were obtained with TLBO algorithm, correlation coefficient being 0.94 for an MLP(6:9:20:2) – a feedforward neural network with two hidden layers and 9 and 20, respectively, intermediate neurons. Good results obtained prove the efficiency of the optimization algorithms. More than the good results, what is important in this approach is the simulation methodology, including neural networks and optimization biologically inspired algorithms, which provide satisfactory results. In addition, the methodology developed in this approach is general and has flexibility so that it can be easily adapted to other processes in association with different types of models.

Keywords: artificial neural networks, human behaviors of learning and cooperation, human competitive behavior, optimization algorithms

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2490 Evolution of DNA-Binding With-One-Finger Transcriptional Factor Family in Diploid Cotton Gossypium raimondii

Authors: Waqas Shafqat Chattha, Muhammad Iqbal, Amir Shakeel

Abstract:

Transcriptional factors are proteins that play a vital role in regulating the transcription of target genes in different biological processes and are being widely studied in different plant species. In the current era of genomics, plant genomes sequencing has directed to the genome-wide identification, analyses and categorization of diverse transcription factor families and hence provide key insights into their structural as well as functional diversity. The DNA-binding with One Finger (DOF) proteins belongs to C2-C2-type zinc finger protein family. DOF proteins are plant-specific transcription factors implicated in diverse functions including seed maturation and germination, phytohormone signalling, light-mediated gene regulation, cotton-fiber elongation and responses of the plant to biotic as well as abiotic stresses. In this context, a genome-wide in-silico analysis of DOF TF family in diploid cotton species i.e. Gossypium raimondii has enabled us to identify 55 non-redundant genes encoding DOF proteins renamed as GrDofs (Gossypium raimondii Dof). Gene distribution studies have shown that all of the GrDof genes are unevenly distributed across 12 out of 13 G. raimondii chromosomes. The gene structure analysis illustrated that 34 out of 55 GrDof genes are intron-less while remaining 21 genes have a single intron. Protein sequence-based phylogenetic analysis of putative 55 GrDOFs has divided these proteins into 5 major groups with various paralogous gene pairs. Molecular evolutionary studies aided with the conserved domain as well as gene structure analysis suggested that segmental duplications were the principal contributors for the expansion of Dof genes in G. raimondii.

Keywords: diploid cotton , G. raimondii, phylogenetic analysis, transcription factor

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2489 Application of Innovative Implementations in the SME Sector

Authors: Mateusz Janas

Abstract:

Innovative implementations in the micro, small, and medium-sized enterprises (MSME) sector are among the essential activities considering the current market realities, technological advancements, and digitization trends. MSMEs play a crucial role and significantly influence the economic conditions of countries, as their competitiveness directly impacts the global economy. Business development and investment in innovation and technology are integral parts of every modern enterprise's strategy, seeking to maintain and achieve a desired competitive position. The instability of the socio-economic environment, along with contemporary changes in artificial intelligence implementation and digitization, requires businesses to adopt increasingly newer solutions and actions. Enterprises must strive to survive in the global market and build competitive positions, especially in uncertain conditions. Being aware of the significance of innovative actions is crucial for MSMEs as it enables them to enhance their operations and expand their scope. It is essential for managers and executives of MSMEs to be focused on development and innovation, as their approach will also impact their employees, emphasizing results and maximizing the company's value. Managers of MSMEs must be aware of various threats, costs, opportunities, and gains that can arise from implementing new technical and organizational solutions. Businesses must view development as an integral part of their strategy and continuously strive for improvement.

Keywords: innovation, SME, develop, management

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2488 Comparison of Acetylcholinesterase Reactivators Cytotoxicity with Their Structure

Authors: Lubica Muckova, Petr Jost, Jaroslav Pejchal, Daniel Jun

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The development of acetylcholinesterase reactivators, i.e. antidotes against organophosphorus poisoning, is an important goal of defence research. The aim of this study was to compare cytotoxicity and chemical structure of 5 currently available (pralidoxime, trimedoxime, obidoxime, methoxime, and asoxime) and 4 newly developed compounds (K027, K074, K075, and K203). In oximes, there could be at least four important structural factors affecting their toxicity, including the number of oxime groups in the molecule, the position of oxime group(s) on pyridinium ring, the length of carbon linker, and the substitution by oxygen or insertion of the double bond into the connection chain. The cytotoxicity of tested substances was measured using colorimetric 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-tetrazolium bromide assay (MTT assay) in SH-SY5Y cell line. Toxicity was expressed as toxicological index IC₅₀. The tested compounds showed different cytotoxicity ranging from 1.5 to 27 mM. K027 was the least, and methoxime was the most toxic reactivator. The lowest toxicity was found in a monopyridinium reactivator and bispyridinium reactivators with simple 3C carbon linker. Shortening of connection chain length to 1C, incorporation of oxygen moiety into 3C compounds, elongation of carbon linker to 4C and insertion of a double bond into 4C substances increase AChE reactivators' cytotoxicity. Acknowledgements: This work was supported by a long-term organization development plan Medical Aspects of Weapons of Mass Destruction of the Faculty of Military Health Sciences, University of Defence.

Keywords: acetylcholinesterase, cytotoxicity, organophosphorus poisoning, reactivators of acetylcholinesterase

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