Search results for: in vitro antibacterial activity

Authors: Ceren Akyüz, Ingo Froboese

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Health literacy has gained importance with the further spread of the coronavirus disease (COVID-19) worldwide and has been associated with health status in various chronic diseases. Many studies indicate that mental health can be improved by low- or moderate-intensity activity, and several studies have been proposed to explain the relationship between physical activity and mental health. The aim of the present study is to investigate the levels of physical activity, health literacy, and depression in first- and- second generation Turkish people in Germany. The research consists of 434 participants (255 females, 179 males; age 38.09 ± 13.73). 40.8 % of participants are married, and 59.2 % of participants are single. Education levels are mostly at university level (54.8 %), and graduate level is 18.9 %. While 24.9 % of the participants are second generation, 75.1 % of participants are first generation. All analyses were stratified on gender, marital status, education, generation and income status, and five age categories: 18–30, 31–40, 41–50, 51–60, and 61–79, which were defined to account for age-specific trends while maintaining sufficient cell size for statistical analysis. A correlation of depression with physical activity and health literacy levels between first- and- second generation Turks in Germany was evaluated in order to find out whether there are significant differences between the two populations and demographic variables (gender, marital status, education, generation, income status) with carrying out questionnaires which are European Health Literacy Survey Questionnaire (HLS-EU-Q47), International Physical Activity Questionnaire ( IPAQ) and the Patient Health Questionnaire-9 (PHQ-9).

Keywords: health literacy, turks in germany, migrants, depression, physical activity

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Authors: Zhen Qin, Yufei Peng, Jianbei Li, Jidong Long

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In order to study the activity of the coated aluminate barium-tungsten cathodes during activation, aging, poisoning and long-term use. Through a set of hot-cathode micro-area emission uniformity study device, we tested the micro-area emission performance of the cathode under different conditions. The change of activity of cathode micro-area was obtained. The influence of micro-area activity on the performance of the cathode was explained by the ageing model of barium-tungsten cathode. This helps to improve the design and process of the cathode and can point the way in finding the factors that affect life in the cathode operation.

Keywords: barium-tungsten cathode, ageing model, micro-area emission, emission uniformity

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Authors: Marcela Dvorakova, Lenka Langhansova, Premysl Landa

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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

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Authors: Amel Bouaziz, Seddik Khennouf, Mussa Abu Zarga, Shtayway Abdalla, Saliha Djidel, Assia Bentahar, Saliha Dahamna, Smain Amira

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The present study aimed to evaluate the hypotensive and the in vitro antioxidant activities of Crataegus azarolus L. (Rosaceae), a plant widely used as natural remedy for hypertension in folk medicine. The antioxidant potential of methanolic extract (ME)and its three fractions of Chloroform (CHE), ethyl acetate (EAE)and water (AqE) have been investigated using several assays, including the DPPH scavenging, ABTS scavenging, hydroxyl radical scavenging. Inhibition of lipid peroxidation was performed by the β-carotene bleaching assay, ferric thiocyanate method and thiobarburic acid method. Total phenolic and total flavonoid contents of the extracts were estimated using Folin-Chiocalteu reagent and AlCl3, respectively. EAE extract showed the highest polyphenolic and flavonoids contents (396,04±1.20 mg GAE/g of dry extract and 32,73 ± 0.03mg QE/g of dry extract) respectively. Similarly, this extract possessed the highest scavenging activity for DPPH radical (IC 50 = 0,006±0,0001mg /ml), ABTS radical (IC50=0.0035±0,0007 mg/ml) and hydroxyl radical(IC 50=0,283± 0.01 mg/ml). In addition, the EAE exhibited the highest antioxidant activity in the inhibition of linoleic acid/ß-carotene coupled oxidation (89,21%), lipid peroxidation in the ferric thiocyanate(FTC) method (90.13%), and thio-barbituric acid (TBA) method (74.23%). Intravenous administration of Me and EAE decreased mean arterial blood pressure, systolic and diastolic blood pressure in anesthetized rats dose-dependently, at the dose range of 0.4 to 12 mg/kg. The mean arterial blood pressure dropped by 27.58 and 39.37% for ME and EAE, respectively. In conclusion, The present study supported the significant potential to use C. azarolus by-products as a source of natural antioxidants and provides scientific justification for its traditional uses as cardio-protective and anti-hypertensive remedy.

Keywords: Crataegus azarolus, polyphenols, flavonoids, hypertension, antioxidant activity, free radicals, peroxidation

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Authors: M. Rodionov, Z. Dedovets

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This article discusses ways to implement a differentiated approach to developing academic motivation for mathematical studies which relies on defining the primary structural characteristics of motivation. The following characteristics are considered: features of realization of cognitive activity, meaning-making characteristics, level of generalization and consistency of knowledge acquired by personal experience. The assessment of the present level of individual student understanding of each component of academic motivation is the basis for defining the relevant educational strategy for its further development.

Keywords: learning activity, mathematics, motivation, student

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Authors: Tesfay Gebremichael Reda

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Nanoparticle technology is fast progressing and is being employed in innumerable medical applications. At this time, the public's health is seriously threatened by the rise of bacterial strains resistant to several medications. Metal nanoparticles are a potential alternate approach for tackling this global concern, and this is the main focus of this study. The citrate precursor sol-gel synthesis method was used to synthesize the, Niₓ Co(₁-ₓ) Fe₂ O₄, (where x = 0.0:0.2:1.0) nanoparticle. XRD identified the development of the cubic crystal structure to have a preferential orientation along (311), and the average particle size was found to be 29-38 nm. The average crystallizes assessed with ImageJ software and origin 22 of the SEM are nearly identical to the XRD results. In the created NCF NPs, the FT-IR spectroscopy reveals structural examinations and the redistribution of cations between octahedral (505-428 cm-1) and tetrahedral (653-603 cm-1) locales. Finally, the decrease of coercive fields HC, 2384 Oe to 241.93 Oe replacement of Co²+ cation with Ni²+. Band gap energy rises as Ni concentration increases, which may be attributed to the fact that the ionic radii of Ni²+ ions are smaller than that of Co²+ ions, which results in a strong electrostatic interaction. On the contrary, except at x = 0.4, the dielectric constant decreases as the nickel concentration increases. According to the findings of this research work, nanoparticles composed of Ni₀.₄ Co₀.₄ Fe₂ O₄ have demonstrated a promising value against S. aureus and E. coli, and it suggests a proposed model for their potential use as a new source of antibacterial agents.

Keywords: antimicrobial, band gap, citrate precursor, dielectric, nanoparticle

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Authors: Caroline Dupre, David Hupin, Christ Goumou, Francois Belan, Frederic Roche, Thomas Celarier, Bienvenu Bongue

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Background: Previous cohorts have been notably criticized for not studying the different type of physical activity and not investigating household activities. The objective of this work was to analyse the relationship between physical activity and cognitive decline in older people living in the community. Impact of type of physical activity on the results has been realised. Methods: The study used data from the longitudinal and observational study , FrèLE (FRagility: Longitudinal Study of Expressions). The collected data included: socio-demographic variables, lifestyle, and health status (frailty, comorbidities, cognitive status, depression). Cognitive decline was assessed by using: Mini-Mental State Examination (MMSE) and Montreal Cognitive Assessment (MoCA). Physical activity was assessed by the Physical Activity Scale for the Elderly (PASE). This tool is structured in three sections: the leisure activity, domestic activity, and professional activity. Logistic regressions and proportional hazards regression models (Cox) were used to estimate the risk of cognitive disorders. Results: At baseline, the prevalence of cognitive disorders was 6.9% according to MMSE. In total, 1167 participants without cognitive disorders were included in the analysis. The mean age was 77.4 years, and 52.1% of the participants were women. After a 2 years long follow-up, we found cognitive disorders on 53 participants (4.5%). Physical activity at baseline is lower in older adults for whom cognitive decline was observed after two years of follow-up. Subclass analyses showed that leisure and domestic activities were associated with cognitive decline, but not professional activities. Conclusions: Analysis showed a relationship between cognitive disorders and type of physical activity. The current study will be completed by the MoCA for mild cognitive impairment. These findings compared to other ongoing studies, will contribute to the debate on the beneficial effects of physical activity on cognition.

Keywords: aging, cognitive function, physical activity, mixed models

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Authors: Likewin Thomas, M. V. Manoj Kumar, B. Annappa

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Traditional execution process follows the path of execution drawn by the process analyst without observing the behaviour of resource and other real-time constraints. Identifying process model, predicting the behaviour of resource and recommending the optimal path of execution for a real time process is challenging. The proposed AlfyMiner: αyM iner gives a new dimension in process execution with the novel techniques Process Model Analyser: PMAMiner and Resource behaviour Analyser: RBAMiner for recommending the probable path of execution. PMAMiner discovers next probable activity for currently executing activity in an online process using variant matching technique to identify the set of next probable activity, among which the next probable activity is discovered using decision tree model. RBAMiner identifies the resource suitable for performing the discovered next probable activity and observe the behaviour based on; load and performance using polynomial regression model, and waiting time using queueing theory. Based on the observed behaviour αyM iner recommend the probable path of execution with; next probable activity and the best suitable resource for performing it. Experiments were conducted on process logs of CoSeLoG Project1 and 72% of accuracy is obtained in identifying and recommending next probable activity and the efficiency of resource performance was optimised by 59% by decreasing their load.

Keywords: cross-organization process mining, process behaviour, path of execution, polynomial regression model

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Authors: Sandhya Parameswaran, Prajakta Dhuri

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Despite great improvements in health care, the world oral health report states that dental problems still persist, particularly among underprivileged groups in both developing and developed countries. Dental caries and periodontal diseases are identified as the most important oral health problems globally. Acidic foods and beverages can affect natural teeth, and chronic exposure often leads to the development of dental erosion, abrasion, and decay. In recent years, there has been an increased interest toward essential oils. These are secondary metabolites and possess antibacterial, antifungal and antioxidant properties. Essential oils are volatile and chemically unstable in the presence of air, light, moisture and high temperature. Hence many novel methods like a liposomal encapsulation of oils have been introduced to enhance the stability and bioavailability. This research paper focuses on two essential oils, clove and cinnamon oil. Clove oil was obtained from Syzygium aromaticum Linn using clavengers apparatus. It contains eugenol and β caryophyllene. Cinnamon oil, from the barks of Cinnamomum cassia, contains cinnamaldehyde, The objective of the current research was to develop a liposomal carrier system containing clove and cinnamon oil and study their synergistic activity against dental pathogens when formulated as a gel. Methodology: The essential oil were first tested for their antimicrobial activity against dental pathogens, Lactobacillus acidophillus (MTCC No. 10307, MRS broth) and Streptococcus Mutans (MTCC No .890, Brain Heart Infusion agar). The oils were analysed by UV spectroscopy for eugenol and cinnamaldehyde content. Standard eugenol was linear between 5ppm to 25ppm at 282nm and standard cinnamaldehde from 1ppm to 5pmm at 284nm. The concentration of eugenol in clove oil was found to be 62.65 % w/w, and that of cinnamaldehyde was found to be 5.15%s w/w. The oils were then formulated into liposomes. Liposomes were prepared by thin film hydration method using Phospholipid, Cholesterol, and other oils dissolved in a chloroform methanol (3:1) mixture. The organic solvent was evaporated in a rotary evaporator above lipid transition temperature. The film was hydrated with phosphate buffer (pH 5.5).The various batches of liposomes were characterized and compared for their size, loading rate, encapsulation efficiency and morphology. The prepared liposomes when evaluated for entrapment efficiency showed 65% entrapment for clove and 85% for cinnamon oil. They were also tested for their antimicrobial activity against dental pathogens and their synergistic activity studied. Based on the activity and the entrapment efficiency the amount of liposomes required to prepare 1gm of the gel was calculated. The gel was prepared using a simple ointment base and contained 0.56% of cinnamon and clove liposomes. A simultaneous method of analysis for eugenol and cinnamaldehyde.was then developed using HPLC. The prepared gels were then studied for their stability as per ICH guidelines. Conclusion: It was found that liposomes exhibited spherical shaped vesicles and protected the essential oil from degradation. Liposomes, therefore, constitute a suitable system for encapsulation of volatile, unstable essential oil constituents.

Keywords: cinnamon oil, clove oil, dental caries, liposomes

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Authors: H. Pegram, R. Stevens, L. De Girolamo

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Aligned electrospun nanofibres act as effective neuronal and glial cell scaffolds that can be layered to contain multiple sheets harboring different cell populations. This allows personalised biofunctional prostheses to be manufactured with both acellular and cellularised layers for the treatment of spinal cord injury. Additionally, the manufacturing route may be configured to produce in-vitro 3D cell based model of spinal cord injury to aid drug development and enhance prosthesis performance. The goal of this investigation was to optimise the multi-layer scaffold design parameters for prosthesis manufacture, to enable the development of multi-layer patient specific implant therapies. The work has also focused on the fabricating aligned nanofibre scaffolds that promote in-vitro neuronal and glial cell population growth, cell-to-cell interaction and long-term survival following trauma to mimic an in-vivo spinal cord lesion. The approach has established reproducible lesions and has identified markers of trauma and regeneration marked by effective neuronal migration across the lesion with glial support. The investigation has advanced the development of an in-vitro model of traumatic spinal cord injury and has identified a route to manufacture prostheses which target the repair spinal cord injury. Evidence collated to investigate the multi-layer concept suggests that physical cues provided by nanofibres provide both a natural extra-cellular matrix (ECM) like environment and controls cell proliferation and migration. Specifically, aligned nanofibre layers act as a guidance system for migrating and elongating neurons. On a larger scale, material type in multi-layer systems also has an influence in inter-layer migration as cell types favour different material types. Results have shown that layering nanofibre membranes create a multi-level scaffold system which can enhance or prohibit cell migration between layers. It is hypothesised that modifying nanofibre layer material permits control over neuronal/glial cell migration. Using this concept, layering of neuronal and glial cells has become possible, in the context of tissue engineering and also modelling in-vitro induced lesions.

Keywords: electrospinning, layering, lesion, modeling, nanofibre

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Authors: Salama A. Ouf, Amera A. El-Adly, Abdelaleam H. Mohamed

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Dermatophytosis is the infection of keratinized tissues such as hair, nail and the stratum corneum of the skin by dermatophytic fungi. Infection is generally cutaneous and restricted to the non-living cornified layers because of the inability of the fungi to penetrate the deeper tissues or organs of immunocompetent hosts. In Saudi Arabia, Onychomycosis is the most frequent infection (40.3%), followed by tinea capitis (21.9%), tinea pedis (16%), tinea cruris (15.1%), and tinea corporis (6.7%). Several azole compounds have been tried to control dermatophytic infection, however, the azole-containing medicines may interfere with the activity of hepatic microsomal enzymes, sex and thyroid hormones, and testosterone biosynthesis. In this research, antibody-conjugated nanoparticles stimulated by cold plasma and laser were evaluated in vitro against some dermatophytes isolated from the common types of tinea. Different types of nanomaterials were tested but silver nanoparticles (AgNPs) were proved to be most effective against the dermatophytes under test. The use of cold plasma coupled with antibody-conjugated nano-particles has severe impact on dermatophytes where the inhibition of growth, spore germination keratinase activity was more than 88% in the case of Trichophyton rubrum, T. violaceum, Microsprum canis and M. gypseum. Complete inhibition of growth for all dermatophytes was brought about by the interaction of conjugated nanoparticles, with cold plasma and laser treatment. The in vivo test with inoculated guinea pigs achieved promising results where the recovery from the infection reached 95% in the case of M. canis –inoculated pigs treated with AgNPs pretreated with cold plasma and laser.

Keywords: cold plasma, dermatophytes, laser, silver nanoparticles

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Authors: Paresh M. Patel, Amit A. Patel, R. H. Parikh

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The present investigation was undertaken to fabricate modified transport fluconazole that belongs to BCS class II and have a poor applicability on topical infection. So to improve topical application, transdermal spray could play a vital role by using ethyl cellulose and Eudragit® S100 as film-forming polymers. Concentration of Eudragit® S100, ethyl cellulose and permeation enhancer (camphor and menthol) were selected as independent variables, whereas drying time, viscosity and in-vitro drug release were selected as dependent variables in factorial design. The viscosity, drying time and in-vitro drug release of the optimize batch B15 was 40.1 cps, 47 sec. and 90.79% respectively. The film of optimized batch was flexible and dermal-adhesive.

Keywords: Eudragit, ethyl cellulose, fluconazole, transdermal spray

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Authors: Anurag Kumar Pandey, Tapan Kumar Nath, Santanu Dhara

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Polluted water by industrial effluents or dyes has become a major global concern, particularly in developing countries. Such environmental contaminants constitute a serious threat to biodiversity, ecosystems, and human health worldwide; thus, their treatment is critical. The usage of nanoparticles has been discovered to be a potential water treatment method with high efficiency, cheap manufacturing costs, and green synthesis. Carbon dots have attracted the interest of researchers due to their unique properties, such as high water solubility, ease of production, great electron-donating ability, and low toxicity. In this context, we synthesized iodine-doped clove buds-derived carbon dots (I-CCDs) for the Fenton-like degradation of environmental contaminants in water (such as methylene blue (MB) and rhodamine-B (Rh-B) dye). The formation of I-CCDs has been confirmed using various spectroscopy techniques. I-CCDs have demonstrated remarkable optical, cytocompatibility, and antibacterial capabilities. The C-dots that were synthesized were found to be an effective catalyst for the reduction of MB and Rh-B utilizing NaBH4 as a reducing agent. UV-visible spectroscopy was used to construct a detailed pathway for dye reduction step by step. As-prepared I-CCDs have the potential to be a promising solution for wastewater purification and treatment systems.

Keywords: iodine-doped carbon dots, wastewater treatment and purification, environmental friendly, antibacterial

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Authors: Salman Ali Nisar, Koshi Suzuki

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Precedence Diagram Method (PDM) with its additional relationships i.e., start-to-start, finish-to-finish, and start-to-finish, between activities provides more flexible schedule than traditional Critical Path Method (CPM). But, changing the duration of critical activities in PDM network will have anomalous effect on critical path. Researchers have proposed some classification of critical activity effects. In this paper, we do further study on classifications of critical activity effect and provide more information in detailed. Furthermore, we determine the maximum amount of time for each class of critical activity effect by which the project managers can control the dynamic feature (shortening/lengthening) of critical activities and project duration more efficiently.

Keywords: construction project management, critical path method, project scheduling, precedence diagram method

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Authors: Rakesh Kumar, Shashi Janeoo, Ankit Dhiman, Siddharth Chopra

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Arynes are versatile reactive intermediates that offer broad opportunities in green organic synthesis. Arynes are potential aryl group surrogates for the transition metal-free environment friendly arylation reactions. Regioselective arylations of quinolines were achieved by the reactions of quinoline N-oxides with aryne intermediates generated in situ from the Kobayashi precursors. Various 2-substituted quinolines provided 3-arylated-2-substituted quinolines under ambient conditions. Acridine N-oxides also reacted well and provided unusual 4-arylacridines. Various fluorine containing 2,3-diarylquinaolines prepared using this approach were evaluated for antibacterial activity and two compounds inhibited the drug-resistant strains of S-aureus with a good selectivity index. Further, the 2,3-diarylquinolines as the potential optoelectronic materials were prepared by the aryne chemistry approach and their optical and electronic properties for such applications are under study. The aryne intermediates provide an effective Green Chemistry tool to achieve versatile arylated heteroarenes for diverse applications.

Keywords: arynes, arylation, quinolines, acridines.

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Authors: Yanting Cao, Kazumitsu Nawata

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As smartphones upgrading, their software and hardware are getting smarter, so the smartphone-based human activity recognition will be described as more refined, complex, and detailed. In this context, we analyzed a set of experimental data obtained by observing and measuring 30 volunteers with six activities of daily living (ADL). Due to the large sample size, especially a 561-feature vector with time and frequency domain variables, cleaning these intractable features and training a proper model becomes extremely challenging. After a series of feature selection and parameters adjustment, a well-performed SVM classifier has been trained.

Keywords: smart sensors, human activity recognition, artificial intelligence, SVM

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Authors: Amer Momani, Tarek Al-Hawari, Abdallah Alakayleh

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This study explains how to construct an actionable activity-based costing and management system to accurately track and account the total costs of architectural aluminum projects. Two ABC models were proposed to accomplish this purpose. First, the learning and development model was introduced to examine how to apply an ABC model in an architectural aluminum firm for the first time and to be familiar with ABC concepts. Second, an actual ABC model was built on the basis of the results of the previous model to accurately trace the actual costs incurred on each project in a year, and to be able to provide a quote with the best trade-off between competitiveness and profitability. The validity of the proposed model was verified on a local architectural aluminum company.

Keywords: activity-based costing, activity-based management, construction, architectural aluminum

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Authors: Bernard L. Middleton, Susan P. Cosgrove

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There is an immediate need for alternative anti-herpetic treatment options effective for both primary infections and reoccurring reactivations of herpes simplex virus types 1 (HSV-1) and 2 (HSV-2). Alternatives currently approved for the purposes of clinical administration includes antivirals and a reduced set of nucleoside analogues. The present article tests a treatment based on a systemic understanding of how the herpes virus affects cell inhibition and breakdown and targets different phases of the viral cycle, including the entry stage, reproductive cross mutation, and cell-to-cell infection. The treatment consisted of five immunotherapeutic core compounds (5CC), which were hypothesized to be capable of neutralizing human monoclonal antibodies. The tested 5CC were noted as being functional in the application of eliminating the DNA synthesis of herpes viral interferon (IFN) - induced cellular antiviral response. They were here found to neutralize antiviral reproduction by blocking cell-to-cell infection. The activity of the 5CC was tested on RC-37 in vitro using an assay plaque reduction and in vivo against HSV-1 and HSV-2. The 50% inhibitory concentration (IC50) of 5CC was 0.0009% for HSV-1 plaque formation and 0.0008% for HSV-2 plaque formation. Further tests were performed to evaluate the susceptibility of HSV-1 and HSV-2 to anti-herpetic drugs in Vero cells after virus entry. There were high-level markers of the 5CC virucidal activity in the viral suspension of HSV-1 and HSV-2. These concentrations of the 5CC are nontoxic and reduced plaque formation by 98.2% for HSV-1 and 93.0% for HSV-2. Virus HSV-1 and HSV-2 titers were reduced significantly by 5CC to the point of being negative, ranging 0.01–0.09 in 72%. The results concluded the 5CC as being an effective treatment option for the herpes simplex virus.

Keywords: synergy pharmaceuticals, herpes treatment, herpes cure, synergy pharmaceuticals treatment

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Authors: Tanju Teker, Yener Tekeli̇, Esra Karpuz

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Salvia species are known as medicinal plant and often used in public. The antimicrobial effects and essential oil composition of Salvia verticillata L. subsp. amasiaca were determined. The antimicrobial activity is determined by using disk diffusion method against two Gram-positive bacteria, two Gram-negative bacteria and one kind of yeast and essential oil composition was determined by GC - MS. As a result of antimicrobial analysis while sample has shown very strong antimicrobial activity against Staphylococcus aureus, moderately effective against Pseudomonas aeruginosa and low effective against Enterococcus faecalis, it has not shown antimicrobial activity against Escherichia coli and C. albicans. Trans-caryophyllene (% 35.07), germacrene-d (% 10.98) and caryopyllene oxide (% 5.81) are the main components of essential oil composition.

Keywords: salvia, medicinal plant, antimicrobial activity, essential oil

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Authors: Sandy Van Vuuren, Lerato Kose, Annah Moteetee

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Lesotho, a country surrounded by South Africa has one of the highest rates of sexually transmitted infections (STI’s) in the world. In fact, the country ranks third highest with respect to infections related to the human immunodeficiency virus (HIV). Despite the high prevalence of STI’s, treatment has been a challenge due to limited accessibility to health facilities. An estimated 77% of the population lives in rural areas and more than 60% of the country is mountainous. Therefore, many villages remain accessible only by foot or horse-back. Thus, the Basotho (indigenous people from Lesotho) have a rich cultural heritage of plant use. The aim of this study was to determine what plant species are used for the treatment of STI’s and which of these have in vitro efficacy against pathogens such as Candida albicans, Gardnerella vaginalis, Oligella ureolytica, and Neisseria gonorrhoeae. A total of 34 medicinal plants were reported by traditional practitioners for the treatment of STI’s. Sixty extracts, both aqueous and organic (mixture of methanol and dichloromethane), from 24 of the recorded plant species were assessed for antimicrobial activity using the minimum inhibition concentration (MIC) micro-titre plate dilution assay. Neisseria gonorrhoeae (ATCC 19424) was found to be the most susceptible among the test pathogens, with the majority of the extracts (21) displaying noteworthy activity (MIC values ≤ 1 mg/ml). Helichrysum caespititium was found to be the most antimicrobially active species (MIC value of 0.01 mg/ml). The results of this study support, to some extent, the traditional medicinal uses of the evaluated plants for the treatment of STI’s, particularly infections related to gonorrhoea.

Keywords: Africa, Candida albicans, Gardnerella vaginalis, Neisseria gonorrhoeae, Oligella urealytica

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Authors: Ya-Lin Chang, Chia Chen Chang, Yu-Ru Liang, Joyce Chen, You-Kang Chang, Tina Chiu

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Physical activity and mental health status are important for health. The purpose of this study was to examine levels of physical activities and depression in Taiwanese vegetarians (VEG) and omnivores (OMNI). Sixty-three vegetarians (20 males) and 56 omnivores (23 males) with an average age of 51 years were recruited for a food frequency validation study at Taipei Tzu Chi Hospital from July to September in 2016. Participants filled out a validated Chinese version international physical activity questionnaire-short-form (IPAQ), Beck Depression Inventory-II-Chinese version (BDI), food frequency questionnaire (FFQ) and a questionnaire on demographics and medical history upon recruitment. Total BDI scores were calculated for depression and the metabolic equivalent of task (MET) was calculated for physical activity levels. Mann-Whitney U tests and Chi-square test were used to compare demographics, physical activity levels and depression scores. VEG and OMNI did not differ significantly on MET (1441.9 ± 3387.3 vs. 1605.8 ± 2486.1. p=0.2652, respectively). VEG scored slightly lower on BDI compared to OMNI without statistical significance (5.6 ± 5.7 vs. 7.4 ± 6.3. p=0.06). In addition, we found that regardless of diet practice, those who held a college degree and above scored better on MET (1788.1 ± 2532.6 vs. 1215.5 ± 3425.5. p=0.0014) and BDI (5.2 ± 5.1 vs. 7.8 ± 6.7. p=0.03). In this cross-sectional study, Taiwanese vegetarians and omnivores scored comparatively on physical activity levels and depression. However, education is a significant determinant of physical activity and depression.

Keywords: BDI, diet, education, physical activity

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Authors: B. Kabane, G. G. Redhi

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An ammonium based ionic liquid (methyltrioctylammonium chloride) [N_{8 8 8 1}] [Cl] was investigated as an extraction potential solvent for volatile organic solvents (in this regard, solutes), which includes alkenes, alkanes, ketones, alkynes, aromatic hydrocarbons, tetrahydrofuran (THF), alcohols, thiophene, water and acetonitrile based on the experimental activity coefficients at infinite THF measurements were conducted by the use of gas-liquid chromatography at four different temperatures (313.15 to 343.15) K. Experimental data of activity coefficients obtained across the examined temperatures were used in order to calculate the physicochemical properties at infinite dilution such as partial molar excess enthalpy, Gibbs free energy and entropy term. Capacity and selectivity data for selected petrochemical extraction problems (heptane/thiophene, heptane/benzene, cyclohaxane/cyclohexene, hexane/toluene, hexane/hexene) were computed from activity coefficients data and compared to the literature values with other ionic liquids. Evaluation of activity coefficients at infinite dilution expands the knowledge and provides a good understanding related to the interactions between the ionic liquid and the investigated compounds.

Keywords: separation, activity coefficients, methyltrioctylammonium chloride, ionic liquid, capacity

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Authors: Nagasamy Venkatesh Dhandapani

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This work aims at investigating the use of β-Cyclodextrin as a cross linker, in an attempt to formulate nanosponges containing ketoconazole. The nanosponges were prepared by cross-linking method. The excipients used in this study did not alter the physicochemical properties of a drug as revealed by FTIR spectroscopy. Studies on various formulation variables revealed that all the variables are inter-related with the formulation. The ideal batch among the formulation was selected based on the higher entrapment efficiency and drug loading. The in vitro release studies of ketoconazole nanosponges in hydrogel exhibited a sustained release over a period of 24 hours. Mathematical analysis of drug release from the formulation followed non-Fickian diffusion obeying first order kinetics. The anti-fungal activity of the formulation exhibited better zone of inhibition when compared to pure drug (ketoconazole) against Tinea corporis.

Keywords: nanosponges, beta-cyclodextrin, ketoconazole, tinea corporis

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Authors: Vinaya Kambappa, Chinnadurai Mani, Komaraiah Palle

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Non-small cell-lung cancer (NSCLC) cells have increased expression of EGFR, which makes them a potential target for cancer therapy. Based on molecular docking and previous reports, we designed and synthesized quinazoline derivatives as potent EGFR inhibitors. Among the derivatives, three compounds showed good antiproliferative activity against A-549 and H-1299 cells. Furthermore, these compounds inhibited EGFR signaling exhibiting diminishing p-EGFR and its downstream proteins like p-Akt, p-Erk1/2, and p-mTOR; however, it did not alter the levels of EGFR, Akt, Erk1/2 and mTOR proteins. Flow cytometric analysis indicated the accumulation of cells at G1 phase suggesting induction of apoptosis, which was further confirmed by annexin V/propidium iodide staining. Our study suggested that quinazoline scaffold can be developed as novel EGFR kinase inhibitors for cancer therapy.

Keywords: apoptosis, non-small cell-lung cancer cells, EGFR, quinazoline

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Authors: Jeena Gupta

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In the today’s world of pharmaceutical products, one should not forget the healing properties of inexpensive food materials especially spices. They are known to possess hidden pharmaceutical ingredients, imparting them the qualities of being anti-microbial, anti-oxidant, anti-inflammatory and anti-carcinogenic. Further aberrant epigenetic regulatory mechanisms like DNA methylation, histone modifications or altered microRNA expression patterns, which regulates gene expression without changing DNA sequence, contribute significantly in the development of various diseases. Changing lifestyles and diets exert their effect by influencing these epigenetic mechanisms which are thus the target of dietary phytochemicals. Bioactive components of plants have been in use since ages but their potential to reverse epigenetic alterations and prevention against diseases is yet to be explored. Spices being rich repositories of many bioactive constituents are responsible for providing them unique aroma and taste. Some spices like curcuma and garlic have been well evaluated for their epigenetic regulatory potential, but for others, it is largely unknown. We have evaluated the biological activity of phyto-active components of Fennel, Cardamom and Fenugreek by in silico molecular modeling, in vitro and in vivo studies. Ligand-based similarity studies were conducted to identify structurally similar compounds to understand their biological phenomenon. The database searching has been done by using Fenchone from fennel, Sabinene from cardamom and protodioscin from fenugreek as a query molecule in the different small molecule databases. Moreover, the results of the database searching exhibited that these compounds are having potential binding with the different targets found in the Protein Data Bank. Further in addition to being epigenetic modifiers, in vitro study had demonstrated the antimicrobial, antifungal, antioxidant and cytotoxicity protective effects of Fenchone, Sabinene and Protodioscin. To best of our knowledge, such type of studies facilitate the target fishing as well as making the roadmap in drug design and discovery process for identification of novel therapeutics.

Keywords: epigenetics, spices, phytochemicals, fenchone

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Authors: G. Eom, H. Kim, A. Hwang, T. Kang, B. Kim

Abstract:

Telomerase activity is overexpressed in over 85% of human cancers while suppressed in normal somatic cells. Telomerase has been attracted as a universal cancer biomarker. Therefore, the development of effective telomerase activity detection methods is urgently demanded in cancer diagnosis and therapy. Herein, we report a nanogap-rich Au nanowire (NW) surface-enhanced Raman scattering (SERS) sensor for detection of human telomerase activity. The nanogap-rich Au NW SERS sensors were prepared simply by uniformly depositing nanoparticles (NPs) on single-crystalline Au NWs. We measured SERS spectra of methylene blue (MB) from 60 different nanogap-rich Au NWs and obtained the relative standard deviation (RSD) of 4.80%, confirming the superb reproducibility of nanogap-rich Au NW SERS sensors. The nanogap-rich Au NW SERS sensors enable us to detect telomerase activity in 0.2 cancer cells/mL. Furthermore, telomerase activity is detectable in 7 different cancer cell lines whereas undetectable in normal cell lines, which suggest the potential applicability of nanogap-rich Au NW SERS sensor in cancer diagnosis. We expect that the present nanogap-rich Au NW SERS sensor can be useful in biomedical applications including a diverse biomarker sensing.

Keywords: cancer biomarker, nanowires, surface-enhanced Raman scattering, telomerase

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Authors: Katarzyna Kwiatkowska, Izabela Walasik, Katarzyna Kosińska-Kaczyńska, Olga Płaza, Kinga Żebrowska

Abstract:

Introduction Adequate physical activity of a pregnant woman has been proven to decrease the risk of pregnancy complications. The knowledge of women regarding physical exercise in pregnancy is a part of conscious motherhood, while a lack of it may lead to not taking up any form of physical activity during pregnancy. Aim: The aim of the study was to assess the knowledge and experience of women regarding physical activity during their latest pregnancy. Material and methodology: An anonymous questionnaire, consisting of 57 questions, was completed electronically in 2018 by women who gave birth at least once. The respondents were qualified as 'physically active during pregnancy' if they performed physical exercises such as regular walks, marching, jogging, working out at a gym, swimming, yoga, pilates, fitness, exercise-ball workouts or home gymnastics. Results: The study group consisted of 9345 women. 52% of them performed exercises during pregnancy. The main reasons for the lack of physical activity were: lack of interest in physical activity (45%), lack of energy (40%), lack of knowledge regarding proper exercise during pregnancy (34%), lack of time (27%) and medical contraindications (25%). Non-active respondents suffered from gestational hypertension (6,7% vs 9,2%; p<00,1) and gave birth prematurely (11% vs 15%; p < 001) to newborns with a lower birth weight significantly more often ( < 2500g vs > 2500g; p < 0,001). Physically active women reported suffering from pregnancy-related ailments such as fatigue, back pain or constipation significantly less often. 22% of all respondents were unable to identify reliable sources of information regarding exercise during pregnancy. A majority of the exercising women used the Internet to obtain gain information on physical activity during pregnancy (69,1%). 4% of women thought that exercising during pregnancy is forbidden, while 20% thought it is not allowed in the 3rd trimester. Physically active women had vaginal delivery more often (61% vs 55%; p < 0,05). Episiotomy was performed most often on non-active primiparous respondents (77,5% vs 71% active primiparous, p < 0,001). 13% of women felt discriminated due to their physical activity during pregnancy. 22% of respondents’ physical activity was not accepted by their environment. 39,1% of the women were told by others to stop physical exercise because it was bad for the baby’s health. Conclusion: The knowledge of Polish women regarding proper physical activity during pregnancy is insufficient, which may influence a lack of will to initiate such activity among pregnant women. Physical activity of a pregnant woman may have an impact on the course of pregnancy and birth.

Keywords: childbirth, discrimination, physical activity, pregnancy

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Authors: Umme Hani, Mohammed Rahmatulla, Mohammed Ghazwani, Ali Alqahtani, Yahya Alhamhoom

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Background and introduction: Neratinib is a potent anticancer drug used for the treatment of breast cancer. It is poorly soluble at higher pH, which tends to minimize the therapeutic effects in the lower gastrointestinal tract (GIT) leading to poor bioavailability. An attempt has been made to prepare and develop a gastro-retentive system of Neratinib to improve the drug bioavailability in the GIT by enhancing the gastric retention time. Materials and methods: In the present study a three-factor at two-level (23) factorial design based optimization was used to inspect the effects of three independent variables (factors) such as sodium alginate (A), sodium bicarbonate (B) and sodium citrate (C) on the dependent variables like in vitro gelation, in vitro floating, water uptake and percentage drug release. Results: All the formulations showed pH in the range 6.7 ±0.25 to 7.4 ±0.24, percentage drug content was observed to be 96.3±0.27 to 99.5 ±0.28%, in vitro gelation observed as gelation immediate remains for an extended period. Percentage of water uptake was in the range between 9.01±0.15 to 31.01±0.25%, floating lag time was estimated form 7±0.39 to 57±0.36 sec. F4 and F5 showed floating even after 12hrs. All formulations showed a release of around 90% drug release within 12hr. It was observed that the selected independent variables affect the dependent variables. Conclusion: The developed system may be a promising and alternative approach to augment gastric retention of drugs and enhances the therapeutic efficacy of the drug.

Keywords: neratinib, 2³ factorial design, sodium alginate, floating, in situ gelling system

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Authors: Sunita Makchuchit, Arunporn Itharat

Abstract:

Prasaprohyai, a Thai traditional medicine preparation listed in the Thai National List of Essential Medicines, is commonly used for treatment of fever and colds. Prasaprohyai preparation consists of 21 different plants, with Kaempferia galanga (50% w/w) as the main ingredient. The objective of this study was to investigate the anti-allergic activity of the crude extract from Prasaprohyai after accelerated stability test procedure. The method of extract used maceration in 95% ethanol and the crude extract was kept under accelerated condition at 40 ± 2 oC and 75 ± 5% relative humidity (RH) for six months. After six months of storage at 40 oC, the crude sample in various storage times (0, 15, 30, 45, 60, 90, 120, 150 and 180 days) were investigated for anti-allergic activity using IgE-sensitized RBL-2H3 cell lines. The results showed that the stability of crude ethanolic extract from Prasaprohyai under accelerated testing had no significant effect of anti-allergic activity when compared with day 0. The results showed that the ethanolic extract could be stored for two years at room temperature without loss of activity.

Keywords: accelerated stability, anti-allergy, prasaprohyai, RBL-2H3 cell lines

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Authors: J. Nisar, S. Halim

Abstract:

The additional relationships i.e., start-to-start, finish-to-finish, and start-to-finish, between activity in Precedence Diagram Method (PDM) provides a more flexible schedule than traditional Critical Path Method (CPM). But, changing the duration of critical activities in the PDM network will have an anomalous effect on the critical path and the project completion date. In this study, we classified the critical activities in two groups i.e., 1. activity on single critical path and 2. activity on multi-critical paths, and six classes i.e., normal, reverse, neutral, perverse, decrease-reverse and increase-normal, based on their effects on project duration in PDM. Furthermore, we determined the maximum float of time by which the duration each type of critical activities can be changed without effecting the project duration. This study would help the project manager to clearly understand the behavior of each critical activity on critical path, and he/she would be able to change the project duration by shortening or lengthening activities based on project budget and project deadline.

Keywords: construction management, critical path method, project scheduling network, precedence diagram method

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