Search results for: cytotoxic activity
6146 Exploiting the Tumour Microenvironment in Order to Optimise Sonodynamic Therapy for Cancer
Authors: Maryam Mohammad Hadi, Heather Nesbitt, Hamzah Masood, Hashim Ahmed, Mark Emberton, John Callan, Alexander MacRobert, Anthony McHale, Nikolitsa Nomikou
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Sonodynamic therapy (SDT) utilises ultrasound in combination with sensitizers, such as porphyrins, for the production of cytotoxic reactive oxygen species (ROS) and the confined ablation of tumours. Ultrasound can be applied locally, and the acoustic waves, at frequencies between 0.5-2 MHz, are transmitted efficiently through tissue. SDT does not require highly toxic agents, and the cytotoxic effect only occurs upon ultrasound exposure at the site of the lesion. Therefore, this approach is not associated with adverse side effects. Further highlighting the benefits of SDT, no cancer cell population has shown resistance to therapy-triggered ROS production or their cytotoxic effects. This is particularly important, given the as yet unresolved issues of radiation and chemo-resistance, to the authors’ best knowledge. Another potential future benefit of this approach – considering its non-thermal mechanism of action – is its possible role as an adjuvant to immunotherapy. Substantial pre-clinical studies have demonstrated the efficacy and targeting capability of this therapeutic approach. However, SDT has yet to be fully characterised and appropriately exploited for the treatment of cancer. In this study, a formulation based on multistimulus-responsive sensitizer-containing nanoparticles that can accumulate in advanced prostate tumours and increase the therapeutic efficacy of SDT has been developed. The formulation is based on a polyglutamate-tyrosine (PGATyr) co-polymer carrying hematoporphyrin. The efficacy of SDT in this study was demonstrated using prostate cancer as the translational exemplar. The formulation was designed to respond to the microenvironment of advanced prostate tumours, such as the overexpression of the proteolytic enzymes, cathepsin-B and prostate-specific membrane antigen (PSMA), that can degrade the nanoparticles, reduce their size, improving both diffusions throughout the tumour mass and cellular uptake. The therapeutic modality was initially tested in vitro using LNCaP and PC3 cells as target cell lines. The SDT efficacy was also examined in vivo, using male SCID mice bearing LNCaP subcutaneous tumours. We have demonstrated that the PGATyr co-polymer is digested by cathepsin B and that digestion of the formulation by cathepsin-B, at tumour-mimicking conditions (acidic pH), leads to decreased nanoparticle size and subsequent increased cellular uptake. Sonodynamic treatment, at both normoxic and hypoxic conditions, demonstrated ultrasound-induced cytotoxic effects only for the nanoparticle-treated prostate cancer cells, while the toxicity of the formulation in the absence of ultrasound was minimal. Our in vivo studies in immunodeficient mice, using the hematoporphyrin-containing PGATyr nanoparticles for SDT, showed a 50% decrease in LNCaP tumour volumes within 24h, following IV administration of a single dose. No adverse effects were recorded, and body weight was stable. The results described in this study clearly demonstrate the promise of SDT to revolutionize cancer treatment. It emphasizes the potential of this therapeutic modality as a fist line treatment or in combination treatment for the elimination or downstaging of difficult to treat cancers, such as prostate, pancreatic, and advanced colorectal cancer.Keywords: sonodynamic therapy, nanoparticles, tumour ablation, ultrasound
Procedia PDF Downloads 1386145 Surface Modified Polyamidoamine Dendrimer with Gallic Acid Overcomes Drug Resistance in Colon Cancer Cells HCT-116
Authors: Khushbu Priyadarshi, Chandramani Pathak
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Cancer cells can develop resistance to conventional therapies especially chemotherapeutic drugs. Resistance to chemotherapy is another challenge in cancer therapeutics. Therefore, it is important to address this issue. Gallic acid (GA) is a natural plant compound that exhibits various biological properties including anti-proliferative, anti-inflammatory, anti-oxidant and anti-bacterial. Despite of the wide spectrum biological properties GA has cytotoxic response and low bioavailability. To overcome this problem, GA was conjugated with the Polyamidoamine(PAMAM) dendrimer for improving the bioavailability and efficient delivery in drug-resistant HCT-116 Colon Cancer cells. Gallic acid was covalently linked to 4.0 G PAMAM dendrimer. PAMAM dendrimer is well established nanocarrier but has cytotoxicity due to presence of amphiphilic nature of amino group. In our study we have modified surface of PAMAM dendrimer with Gallic acid and examine their anti-proliferative effects in drug-resistant HCT-116 cells. Further, drug-resistant colon cancer cells were established and thereafter treated with different concentration of PAMAM-GA to examine their anti-proliferative potential. Our results show that PAMAM-GA conjugate induces apoptotic cell death in HCT-116 and drug-resistant cells observed by Annexin-PI staining. In addition, it also shows that multidrug-resistant drug transporter P-gp protein expression was downregulated with increasing the concentration of GA conjugate. After that we also observed the significant difference in Rh123 efflux and accumulation in drug sensitive and drug-resistant cancer cells. Thus, our study suggests that conjugation of anti-cancer agents with PAMAM could improve drug resistant property and cytotoxic response to treatment of cancer.Keywords: drug resistance, gallic acid, PAMAM dendrimer, P-glycoprotein
Procedia PDF Downloads 1496144 Electronic Physical Activity Record (EPAR): Key for Data Driven Physical Activity Healthcare Services
Authors: Rishi Kanth Saripalle
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Medical experts highly recommend to include physical activity in everyone’s daily routine irrespective of gender or age as it helps to improve various medical issues or curb potential issues. Simultaneously, experts are also diligently trying to provide various healthcare services (interventions, plans, exercise routines, etc.) for promoting healthy living and increasing physical activity in one’s ever increasing hectic schedules. With the introduction of wearables, individuals are able to keep track, analyze, and visualize their daily physical activities. However, there seems to be no common agreed standard for representing, gathering, aggregating and analyzing an individual’s physical activity data from disparate multiple sources (exercise pans, multiple wearables, etc.). This issue makes it highly impractical to develop any data-driven physical activity applications and healthcare programs. Further, the inability to integrate the physical activity data into an individual’s Electronic Health Record to provide a wholistic image of that individual’s health is still eluding the experts. This article has identified three primary reasons for this potential issue. First, there is no agreed standard, both structure and semantic, for representing and sharing physical activity data across disparate systems. Second, various organizations (e.g., LA fitness, Gold’s Gym, etc.) and research backed interventions and programs still primarily rely on paper or unstructured format (such as text or notes) to keep track of the data generated from physical activities. Finally, most of the wearable devices operate in silos. This article identifies the underlying problem, explores the idea of reusing existing standards, and identifies the essential modules required to move forward.Keywords: electronic physical activity record, physical activity in EHR EIM, tracking physical activity data, physical activity data standards
Procedia PDF Downloads 2826143 Positive effect of Cu2+ and Ca2+ on the Thermostability of Bambara Groundnut Peroxidase A6, and its Catalytic Efficiency Toward the Oxidation of 3,3,5,5 -Tetramethyl Benzidine
Authors: Yves Mann Elate Lea Mbassi, Marie Solange Evehe Bebandoue, Wilfred Fon Mbacham
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Improving the catalytic performance of enzymes has been a long-standing theme of analytical biochemistry research. Induction of peroxidase activity by metals is a common reaction in higher plants. We thought that this increase in peroxidase activity may be due, on the one hand, to the stimulation of the gene expression of these enzymes but also to a modification of their chemical reactivity following the binding of some metal ions on their active site. We tested the effect of some metal salts (MgCl₂, MnCl₂, ZnCl₂, CaCl₂ and CuSO₄) on the activity and thermostability of peroxidase A6, a thermostable peroxidase that we discovered and purified in a previous study. The chromogenic substrate used was 3,3′,5,5′-tetramethylbenzidine. Of all the metals tested for their effect on A6, only magnesium and copper had a significant effect on the activity of the enzyme at room temperature. The Mann-Whitney test shows a slight inhibitory effect of activity by the magnesium salt (P = 0.043), while the activity of the enzyme is 5 times higher in the presence of the copper salt (P = 0.002). Moreover, the thermostability of peroxidase A6 is increased when calcium and copper salts are present. The activity in the presence of CaCl₂ is 8 times higher than the residual activity of the enzyme alone after incubation at 80°C for 10 min and 35 times higher in the presence of CuSO4 under the same conditions. In addition, manganese and zinc salts slightly reduce the thermostability of the enzyme. The activity and structural stability of peroxidase A6 can clearly be activated by Cu₂+, which therefore enhance the oxidation of 3,3′,5,5′-tetramethylbenzidine, which was used in this study as a chromogenic substrate. Ca₂+ likely has a more stabilizing function for the catalytic site.Keywords: peroxidase activity, copper ions, calcium ions, thermostability
Procedia PDF Downloads 756142 Anti-Allergic Activities of Smilax Glabra Rhizome Extracts and Its Isolated Compounds
Authors: Arunporn Itharat, Kamonmas Srikwan, Srisopa Ruangnoo, Pakakrong Thongdeeying
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Background: The rhizomes of Smilax glabra (SG) has long been used in Traditional Chinese and Thai herbal medicine to treat a variety of infectious diseases and immunological disorders. Objective: To investigate the in vitro anti-allergic activities of crude extracts and pure isolated flavonoid compounds from SG by determination of inhibitory effects on antigen-induced release of β-hexosaminidase from RBL-2H3 cells. Methods: The in vitro inhibitory effects of crude aqueous and organic extracts on beta-hexosaminidase release in RBL-2H3 cells were evaluated as an in vitro indication of possible anti-allergic activity in vivo. Bioassay-guided fractionation of extracts was used to isolate flavonoid compounds from the ethanolic extracts. Results: The 95% and 50% ethanolic extracts of SG showed remarkably high anti-allergic activity, with IC50 values of 5.74 ± 2.44 and 23.54 ± 4.75 μg/ml, much higher activity than that for Ketotifen (IC50 58.90 μM). The water extract had negligible activity (IC50 > 100 μg/ml). The two isolated flavonols, Engeletin and Astilbin, showed weak anti-allergic activity, IC50 values 97.46 ± 2.04 and > 100 μg/ml, respectively. Conclusions: The 95% and 50% ethanolic extracts of SG showed strong anti-allergic activity but two flavonol constituents did not show any significant anti-allergic activity. These findings suggest that a combination of effects of various phytochemicals in crude extracts used in traditional medicine are responsible for the purported anti-allergic activity of SG herbal preparations. The plethora of constituents in crude extracts, as yet unidentified, are likely to be acting synergistically to account for the strong observed anti-allergic in vitro activity.Keywords: Smilax glabra, anti-allergic activity, RBL-2H3 cells, flavonoid compounds
Procedia PDF Downloads 6676141 Phytochimical Screening and Antimicrobial Activity of Ethanolic Extract of Solenostemma Argel (Asclepiadaceae)
Authors: Fatma Acheuk, Akila Hamichi, Siham Semmar
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The crude ethanolic extract from Solenostemma argel was obtained by maceration of leaves and stems of the plant. Phytochimical study revealed the richness of the species on flavonoids, alkaloids, tannins and glycosides. Antimicrobial activity of the growth of clinical isolates of Eschirichia coli, Pseudomonas aeriginosa, Staphylococus aureus and Bacillus Subtilis was carried out using agar disc diffusion. The results of the study revealed that the test compound has antimicrobial activity against gram-positive bacteria which are resistant to commonly antimicrobial agents used. However, no effect was observed on other species tested.Keywords: Solenostemma argel, crude extract, phytochemical screening, antimicrobial activity
Procedia PDF Downloads 3826140 The Relationships between Autonomy-Based Insula Activity and Learning: A Functional Magnetic Resonance Imaging Study
Authors: Woogul Lee, Johnmarshall Reeve
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Learners’ perceived autonomy predicts learners’ interest, engagement, and learning. To understand these processes, we conducted an fMRI experiment. In this experiment, participants saw the national flag and were asked to rate how much they freely wanted to learn about that particular national flag. The participants then learned the characteristics of the national flag. Results showed that (1) the degree of participants’ perceived autonomy was positively correlated with the degree of insula activity, (2) participants’ early-trial insula activity predicted corresponding late-trial dorsolateral prefrontal cortex activity, and (3) the degree of dorsolateral prefrontal cortex activity was positively correlated with the degree of participants’ learning about the characteristics of the national flag. Results suggest that learners’ perceived autonomy predicts learning through the mediation of insula activity associated with intrinsic satisfaction and 'pure self' processes.Keywords: insular cortex, autonomy, self-determination, dorsolateral prefrontal cortex
Procedia PDF Downloads 2046139 Activity-Based Costing in the Hospitality Industry: A Case Study in a Hotel
Authors: Bita Mashayekhi, Mohammad Ara
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The purpose of this study is to provide some empirical evidence about implementing Activity-Based Costing (ABC) in the hospitality industry in Iran. For this purpose, we consider the Tabriz International Hotel as our sample hotel and then gather the relevant data from its cost accounting system in 2012. Then, we use ABC as our costing method and compare the cost of each service unit with that cost which had been extracted for the traditional costing method. The results show a different cost per unit for two methods. Also, because of its more precise and detailed provided information, an ABC system facilitates the decision-making process for managers on decisions related to profitability analysis, budgeting, pricing, and so on.Keywords: Activity-Based Costing (ABC), activity, cost driver, hospitality industry
Procedia PDF Downloads 2986138 Identification of Natural Liver X Receptor Agonists as the Treatments or Supplements for the Management of Alzheimer and Metabolic Diseases
Authors: Hsiang-Ru Lin
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Cholesterol plays an essential role in the regulation of the progression of numerous important diseases including atherosclerosis and Alzheimer disease so the generation of suitable cholesterol-lowering reagents is urgent to develop. Liver X receptor (LXR) is a ligand-activated transcription factor whose natural ligands are cholesterols, oxysterols and glucose. Once being activated, LXR can transactivate the transcription action of various genes including CYP7A1, ABCA1, and SREBP1c, involved in the lipid metabolism, glucose metabolism and inflammatory pathway. Essentially, the upregulation of ABCA1 facilitates cholesterol efflux from the cells and attenuates the production of beta-amyloid (ABeta) 42 in brain so LXR is a promising target to develop the cholesterol-lowering reagents and preventative treatment of Alzheimer disease. Engelhardia roxburghiana is a deciduous tree growing in India, China, and Taiwan. However, its chemical composition is only reported to exhibit antitubercular and anti-inflammatory effects. In this study, four compounds, engelheptanoxides A, C, engelhardiol A, and B isolated from the root of Engelhardia roxburghiana were evaluated for their agonistic activity against LXR by the transient transfection reporter assays in the HepG2 cells. Furthermore, their interactive modes with LXR ligand binding pocket were generated by molecular modeling programs. By using the cell-based biological assays, engelheptanoxides A, C, engelhardiol A, and B showing no cytotoxic effect against the proliferation of HepG2 cells, exerted obvious LXR agonistic effects with similar activity as T0901317, a novel synthetic LXR agonist. Further modeling studies including docking and SAR (structure-activity relationship) showed that these compounds can locate in LXR ligand binding pocket in the similar manner as T0901317. Thus, LXR is one of nuclear receptors targeted by pharmaceutical industry for developing treatments of Alzheimer and atherosclerosis diseases. Importantly, the cell-based assays, together with molecular modeling studies suggesting a plausible binding mode, demonstrate that engelheptanoxides A, C, engelhardiol A, and B function as LXR agonists. This is the first report to demonstrate that the extract of Engelhardia roxburghiana contains LXR agonists. As such, these active components of Engelhardia roxburghiana or subsequent analogs may show important therapeutic effects through selective modulation of the LXR pathway.Keywords: Liver X receptor (LXR), Engelhardia roxburghiana, CYP7A1, ABCA1, SREBP1c, HepG2 cells
Procedia PDF Downloads 4206137 Synthesis and Properties of Sulfonate Gemini Surfactants with Amide Groups
Authors: Rui Wang, Shanfa Tang, Yuanwu Dong, Siyao Wang, Zhaowen Jiang, Di Han
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A sulfonate Gemini surfactant sodium N,N`-bis(tetradecanoyl) propanediamine dipropyl sulfonate (GNS-14) was synthesized from 1,3-propanediamine, tetradecanoyl chloride, and1,3-propanesulfonic lactone. GNS-14 was characterized by FT-IR, 1H NMR. The surface activity, interfacial activity, and emulsification properties of GNS-14 solution were systematically studied. The critical micelle concentration (CCMC) of GNS-14 surfactant was 0.056 mmol/L, and the surface tension (γCMC) was 18.2 mN/m; at 50℃, 0.5% GNS-14 solution can reduce the oil-water interfacial tension to 6.5×10−2 mN/m. GNS-14 has excellent surface activity, interfacial activity, and emulsifying properties.Keywords: gemini surfactants, surface tension, low interfacial tension, emulsifying properties
Procedia PDF Downloads 1536136 A Cognitive Schema of Architectural Designing Activity
Authors: Abdelmalek Arrouf
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This article sets up a cognitive schema of the architectural designing activity. It begins by outlining, theoretically, an a priori model of its general cognitive mechanisms. The obtained theoretical framework represents the designing activity as a complex system composed of three interrelated subsystems of cognitive actions: a subsystem of meaning production, one of morphology production and finally a subsystem of navigation between the two formers. A protocol analysis that uses statistical and informational tools is then used to measure the validity of the built schema. The model thus achieved shows that the designer begins by conceiving abstract meanings, which he then translates into shapes. That’s why we call it a semio-morphic model of the designing activity.Keywords: designing actions, model of the design process, morphosis, protocol analysis, semiosis
Procedia PDF Downloads 1726135 Examining the Potential of Linear Parks as Sustainable Development Components
Authors: Andreas Savvides, Chloe Kadi
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The objective of this study is to investigate how the planning and design of open parks within neighborhoods and communities can promote physical activity in order to enhance the health of the local population. An extensive literature review was conducted for studies regarding the relationship between health and physical activity and the park characteristics that can promote physical activity among people. The findings of the literature review were then compared and analysed, in order to identify the main characteristics of urban parks that can promote physical activity and enhance public health. In order to find out how the characteristics identified in the literature were applied in real life, an analysis of three existing parks in three different countries was conducted. The parks, apart from their geographical location, also vary in size and layout. The parks were chosen because they are urban open parks and they include facilities for physical activity.Keywords: urban planning, active living behaviour, open parks, sustainable mobility
Procedia PDF Downloads 1316134 Visualizing Matrix Metalloproteinase-2 Activity Using Extracellular Matrix-Immobilized Fluorescence Resonance Energy Transfer Bioprobe in Cancer Cells
Authors: Hawon Lee, Young-Pil Kim
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Visualizing matrix metalloproteinases (MMPs) activity is necessary for understanding cancer metastasis because they are implicated in cell migration and invasion by degrading the extracellular matrix (ECM). While much effort has been made to sense the MMP activity, but extracellularly long-term monitoring of MMP activity still remains challenging. Here, we report a collagen-bound fluorescent bioprobe for the detection of MMP-2 activity in the extracellular environment. This bioprobe consists of ECM-immobilized part (including collagen-bound protein) and MMP-sensing part (including peptide substrate linked with fluorescence resonance energy transfer (FRET) coupler between donor green fluorescent protein (GFP) and acceptor TAMRA dye), which was constructed through intein-mediated self-splicing conjugation. Upon being immobilized on the collagen-coated surface, this bioprobe enabled efficient long-lasting observation of MMP-2 activity in the cultured cells without affecting cell growth and viability. As a result, the FRET ratio (acceptor/donor) decreased as the MMP2 activity increased in cultured cancer cells. Furthermore, unlike wild-type MMP-2, mutated MMP-2 expression (Y580A in the hemopexin region) gave rise to lowering the secretion of MMP-2 in HeLa. Conclusively, our method is anticipated to find applications for tracing and visualizing enzyme activity.Keywords: collagen, ECM, FRET, MMP
Procedia PDF Downloads 2026133 Antimicrobial, Antioxidant and Enzyme Activities of Geosmithia pallida (KU693285): A Fungal Endophyte Associated with Brucea mollis Wall Ex. Kurz, an Endangered and Medicinal Plant of N. E. India
Authors: Deepanwita Deka, Dhruva Kumar Jha
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Endophytes are the microbes that colonize living, internal tissues of plants without causing any immediate, overt negative effects. Endophytes are rich source of therapeutic substances like antimicrobial, anticancerous, herbicidal, insecticidal, immunomodulatory compounds. Brucea mollis, commonly known as Quinine in Assam, belonging to the family Simaroubaceae, is a shrub or small tree, recorded as endangered species in North East India by CAMP survey in 2003. It is traditionally being used as antimalarial and antimicrobial agent and has antiplasmodial, cytotoxic, anticancer, diuretic, cardiovascular effect etc. Being endangered and medicinal; this plant may host certain noble endophytes which need to be studied in depth. The aim of the present study was isolation and identification of potent endophytic fungi from Brucea mollis, an endangered medicinal plant, to protect it from extinction due to over use for medicinal purposes. Aseptically collected leaves, barks and roots samples of healthy plants were washed and cut into a total of 648 segments of about 2 cm long and 0.5 cm broad with sterile knife, comprising 216 segments each from leaves, barks and roots. These segments were surface sterilized using ethanol, mercuric chloride (HgCl2) and aqueous solution of sodium hypochlorite (NaClO). Different media viz., Czapeck-Dox-Agar (CDA, Himedia), Potato-Dextrose-Agar (PDA, Himedia), Malt Extract Agar (MEA, Himedia), Sabourad Dextrose Agar (SDA, Himedia), V8 juice agar, nutrient agar and water agar media and media amended with plant extracts were used separately for the isolation of the endophytic fungi. A total of 11 fungal species were recovered from leaf, bark and root tissues of B. mollis. The isolates were screened for antimicrobial, antioxidant and enzymatic activities using certain protocols. Cochliobolus geniculatus was identified as the most dominant species. The mycelia sterilia (creamy white) showing highest inhibitory activity against Candida albicans (MTCC 183) was induced to sporulate using modified PDA media. The isolate was identified as Geosmithia pallida. The internal transcribed spacer of rDNA was sequenced for confirmation of the taxonomic identity of the sterile mycelia (creamy white). The internal transcribed spacer r-DNA sequence was submitted to the NCBI (KU693285) for the first time from India. G. pallida and Penicillium showed highest antioxidant activity among all the isolates. The antioxidant activity of G. pallida and Penicillium didn’t show statistically significant difference (P˃0.05). G. pallida, Cochliobolus geniculatus and P. purpurogenum respectively showed highest cellulase, amylase and protease activities. Thus, endopytic fungal isolates may be used as potential natural resource of pharmaceutical importance. The endophytic fungi, Geosmithia pallida, may be used for synthesis of pharmaceutically important natural products and consequently can replace plants hitherto used for the same purpose. This study suggests that endophytes should be investigated more aggressively to better understand the endophyte biology of B. mollis.Keywords: Antimicrobial activity, antioxidant activity, Brucea mollis, endophytic fungi, enzyme activity, Geosmithia pallida
Procedia PDF Downloads 1876132 Sedentary Behaviour and Metabolic Rate among Adults Professionals: An Intervention Approach (E-Mobile)
Authors: Ahsan Ullah
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The aim of this study is to measure the relationship between sedentary behaviour and metabolic rate among adult professionals. An intervention (e-mobile) approach was used for gathered the information from the participants. A total of 40 participants (men = 30, and women = 10) with an average age of (36.53 years ± 8.85) were randomly assigned to an intervention group (n= 20) and control group (n= 20). All the participants completed the Sedentary Behaviour Questionnaire (SBQ) and The International Physical Activity Questionnaire (IPAQ) at baseline and at the end of eight weeks. The participants in the intervention group were given physical activity guidelines targeted at increasing physical activity levels during daily activities. On the other side, the control group was advised to continue with their routine daily physical activity. Statistical analyses, including descriptive statistics and inferential analysis like mean, SD, T-tests, and ANOVA, were used to analyze the data and determine relationships between variables. After analyzing the data, the results showed that significant difference in pre and post metabolic rate scores (1488.31 ± 179.13 to 1468.44 ± 128.19) (f = 10.83, p < 0.000) were noted in the experimental group after eight week. The experimental group increased their walking (863.78 METs per week to 1625.55 METs per week), moderate activity (295 METs per week to 743 METs per week) and vigorous activity (362 METs per week to 1366 METs per week) physical activity (all p<0.001). There were no significant differences observed in any outcome measured before and after eight weeks in the control group. These findings suggest that engaging in physical activity can effectively improve metabolic rate and reduce sedentary behavior among physically active adults.Keywords: sedentary behavior, metabolic rate, adult’s professionals, physical activity
Procedia PDF Downloads 286131 Synthesis and Characterization of Some 1, 2, 3-Triazole Derivatives Containing the Chalcone Moiety and Evaluation for their Antimicrobial and Antioxidant Activity
Authors: Desta Gebretekle Shiferaw, Balakrishna Kalluraya
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Triazoles are basic five-membered ring heterocycles with an unsaturated, six-delocalized electron ring system. Since the dawn of click chemistry, triazoles have represented a functional heterocyclic core that has been the foundation of medicinal chemistry. The compounds with 1,2,3-triazole rings can be used in several fields, including medicine, organic synthesis, polymer chemistry, fluorescent imaging, horticulture, and industries, to name a few. Besides that, they found it to have health applications in the prevention and reduction of the risk of diseases, such as anti-cancer, antimicrobial, antiviral, and anti-inflammatory properties. Here, we present the synthesis of twelve 1,2,3-triazolyl chalcone derivatives (4a–l), which were produced in high yields by coupling substituted aldehydes and triazolyl acetophenone (3a–d) in ethanol. The title products were characterized by physicochemical, infrared, nuclear magnetic resonance, and mass spectral methods. The in vitro tests were used to evaluate the antioxidant and antimicrobial activity of each of the prepared molecules. The preliminary assessment and 2,2-diphenyl-1-picrylhydrazyl activity of the title compounds showed significantly higher antibacterial activity and moderate-to-good antifungal and antioxidant activities compared to their standards. This work presents the synthesis of triazolyl chalcone derivatives and their biological activity. Based on the findings, these compounds could be used as lead compounds in antimicrobial and antioxidant research in the future.Keywords: antibacterial activity, antifungal activity, antioxidant activity, chalcone, 1, 2, 3-triazole
Procedia PDF Downloads 1266130 Emergency Condition Discrimination for Single People Using a CO2 Sensor and Body Detectors
Authors: Taiyo Matsumura, Kota Funabashi, Nobumichi Sakai, Takashi Ono
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The purpose of this research is to construct a watching system that monitors human activity in a room and detects abnormalities at an early stage to prevent unattended deaths of people living alone. In this article, we propose a method whereby highly urgent abnormal conditions of a person are determined by changes in the concentration of CO2 generated from activity and respiration in a room. We also discussed the effects the amount of activity has on the determination. The results showed that this discrimination method is not dependent on the amount of activity and is effective in judging highly urgent abnormal conditions.Keywords: abnormal conditions, multiple sensors, people living alone, respiratory arrest, unattended death, watching system
Procedia PDF Downloads 1376129 Producing Graphical User Interface from Activity Diagrams
Authors: Ebitisam K. Elberkawi, Mohamed M. Elammari
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Graphical User Interface (GUI) is essential to programming, as is any other characteristic or feature, due to the fact that GUI components provide the fundamental interaction between the user and the program. Thus, we must give more interest to GUI during building and development of systems. Also, we must give a greater attention to the user who is the basic corner in the dealing with the GUI. This paper introduces an approach for designing GUI from one of the models of business workflows which describe the workflow behavior of a system, specifically through activity diagrams (AD).Keywords: activity diagram, graphical user interface, GUI components, program
Procedia PDF Downloads 4646128 Antimicrobial Activity of Ilex paraguariensis Sub-Fractions after Liquid-Liquid Partitioning
Authors: Sabah El-Sawalhi, Elie Fayad, Roula M. Abdel-Massih
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Ilex paraguariensis (Yerba Mate) is a medium to large tree commonly consumed by South Americans. Its leaves and stems are associated with different biological activities. The purpose of this study was to evaluate the antibacterial activity of Yerba Mate against Gram-positive and Gram-negative bacterial strains and its action against some resistant bacteria with different resistance profiles. Yerba Mate aqueous extracts were prepared at 70°C for 2 hrs, and the microdilution method was used to determine the minimum inhibitory concentration (MIC). Gram-positive bacteria exhibited a stronger antibacterial activity (MIC ranged between 0.468 mg/mL and 15 mg/mL) than Gram-negative bacteria. Yerba Mate was also extracted with acetone: water (1:1) and then further sub-fractionated with hexane, chloroform, and ethyl acetate. MIC values against Staphylococcus aureus ranged from 0.78 to 2.5 mg/ml for the chloroform fraction, from 1.56 to 3.75 mg/ml for the ethyl acetate fraction, and 0.78 to 1.87 mg/ml for the water fraction. The water fraction also exhibited antibacterial activity against Salmonella species (MIC ranged from 1.56 mg/ml to 3.12 mg/ml). The water fraction exhibited the highest antibacterial activity among all the fractions obtained. More studies are needed to determine the molecule or molecules responsible for this activity.Keywords: antibacterial activity, bacterial resistance, minimum inhibitory concentration, yerba mate
Procedia PDF Downloads 1446127 Screening of Antioxidant Activity of Exopolysaccharides Produced by Lactic Acid Bacteria From Human Origin
Authors: Piña-Ronces Laura Gabriela, Reyes-Escogido María de Lourdes
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Exist a large variability in Exopolysaccharides (EPS) produced by LAB depending on carbon source, they have multiple applications in food industry mainly, but they have become important for the health. In this study, we identified EPS-producing strains belonging to the BAL group; they were previously isolated from humans. After that, we extracted and evaluated the antioxidant activity of EPS produced by all strains. Antioxidant activity was determined by DPPH method using ascorbic acid as standard for both comparison and quantification. 31 strains (51.66 %) produced EPS at concentrations between 451 and 1.561 mg/l, 16 of EPS extracted showed antioxidant effect superior to ascorbic acid at the same concentrations. EPS-producing strains were L. plantarum, L. sp and L. fermentum corresponding to Lactobacillus genus and, E. faecium, E. durans, and E. hirae of Enterococcus genus. Antioxidant activity showed by EPS from 3 strains of L. plantarum and 3 strains of E. faecium was different into specie, while the antioxidant activity determined for EPS obtained from the other strains did not show difference at specie level, but was superior to ascorbic acid. EPS produced by L. plantarum and E. hirae had the best activity, it could be considerate for selection them as a possible new alternative for therapy or treatment of diseases related whit oxidative stress. Further studies about biological functions of EPS have to be conducted for new applications in health.Keywords: oxidative stress, lactic acid bacteria, exopolysaccharides, antioxidant activity
Procedia PDF Downloads 3606126 Antioxidant Extraction from Indonesian Crude Palm Oil and Its Antioxidation Activity
Authors: Supriyono, Sumardiyono, Puti Pertiwi
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Crude palm oil (CPO) is a vegetable oil that came from a palm tree bunch. Palm oil tree was known as highest vegetable oil yield. It was grown across Equatorial County, especially in Malaysia and Indonesia. The greenish red color on CPO was came from carotenoid antioxidant, which could be extracted and use separately as functional food and other purposes as antioxidant source. Another antioxidant that also found in CPO is tocopherol. The aim of the research work is to find antioxidant activity on CPO comparing to the synthetic antioxidant that available in a market. On this research work, antioxidant was extracted by using a mixture of acetone and n. hexane, while activity of the antioxidant extract was determine by DPPH method. The extracted matter was shown that their antioxidant activity was about 45% compare to pure tocopherol and beta carotene.Keywords: antioxidant, , beta carotene, , crude palm oil, , DPPH, , tocopherol
Procedia PDF Downloads 2916125 Variation In Gastrocnemius and Hamstring Muscle Activity During Peak Knee Flexor Torque After Anterior Cruciate Ligament Reconstruction with Hamstring Graft
Authors: Luna Sequier, Florian Forelli, Maude Traulle, Amaury Vandebrouck, Pascal Duffiet, Louis Ratte, Jean Mazeas
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The study's objective is to compare the muscular activity of the flexor knee muscle in patients who underwent an anterior cruciate ligament reconstruction with hamstring autograft and the individuals who have not undergone surgery. Methods: The participants were divided into two groups: a healthy group and an experimental group who had undergone an anterior cruciate ligament reconstruction with a hamstring graft. All participants had to perform a knee flexion strength test on an isokinetic dynamometer. The medial Gastrocnemius, lateral Gastrocnemius, Biceps femoris, and medial Hamstring muscle activity were measured during this test. Each group’s mean muscle activity was tested with statistical analysis, and a muscle activity ratio of gastrocnemius and hamstring muscles was calculated Results: The results showed a significant difference in activity of the medial gastrocnemius (p = 0,004901), the biceps femoris (p = 5,394.10-6), and the semitendinosus muscles (p = 1,822.10-6), with a higher Biceps femoris and Semitendinosus activity for the experimental group. It is however noticeable that inter-subject differences were important. Conclusion: This study has shown a difference in the gastrocnemius and hamstring muscle activity between patients who underwent an anterior cruciate ligament reconstruction surgery and healthy participants. With further results, this could show a modification of muscle activity patterns after surgery which could lead to compensatory behaviors at a return to sport and eventually explain a higher injury risk for our patients.Keywords: anterior cruciate ligament, electromyography, muscle activity, physiotherapy
Procedia PDF Downloads 2416124 Student and Group Activity Level Assessment in the ELARS Recommender System
Authors: Martina Holenko Dlab, Natasa Hoic-Bozic
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This paper presents an original approach to student and group activity level assessment that relies on certainty factors theory. Activity level is used to represent quantity and continuity of student’s contributions in individual and collaborative e‑learning activities (e‑tivities) and is calculated to assist teachers in assessing quantitative aspects of student's achievements. Calculated activity levels are also used to raise awareness and provide recommendations during the learning process. The proposed approach was implemented within the educational recommender system ELARS and validated using data obtained from e‑tivity realized during a blended learning course. The results showed that the proposed approach can be used to estimate activity level in the context of e-tivities realized using Web 2.0 tools as well as to facilitate the assessment of quantitative aspect of students’ participation in e‑tivities.Keywords: assessment, ELARS, e-learning, recommender systems, student model
Procedia PDF Downloads 2626123 Anti-Implantation Activity of Kepel (Stelechocarpus burahol) Pulp Ethanol Extract in Female Mice
Authors: Suparmi, Israhnanto Isradji, Dina Fatmawati, Iwang Yusuf
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Kepel (Stelechocarpus burahol) is one of the traditional plants originating from Indonesia that can be used to prevent pregnancy, launched urine and kidney inflammation. Kepel pulp has compounds alkaloid, triterpenoid, tannin, saponin, and flavonoid, when used will give the hormonal and cytotoxic effect. This study was aimed at evaluating ethanol extract of kepel in vivo for anti-implantation activities. In this experimental study with post test only control group design, 20 female mice were randomly divided into 4 groups. It was divided into the control, the 0,65 mg dose, 1,3 mg dose, and 3,6 mg dose of kepel pulp extract group. The extract soluted in DMSO’s solution and was given 1 ml per mice. The extract was given 10 days before copulation until 18 days of pregnancy. Then, the number of implantation, presence of fetus, and embrio resorbtion were recorded and used to calculate the percentage anti-implantation effect. The results were tested by One-way ANOVA. The mean number of implantation in group control, 0,65 mg;1,3 mg; and 2,6 mg were 5,60±1,14; 6,20± 1,64; 7,60±1,51; 8,00± 1,58, respectively. One way Annova test showed that there is no significant difference in the number of implantation between the group (p > 0,05). The administration of kepel pulp ethanol extract had no effect on the percentage anti-implantation effect and the number of and embrio resorbtion.Keywords: antiimplantation, fetus, Stelechocarpus burahol, flavonoid
Procedia PDF Downloads 4366122 Analyzing the Association between Physical Activity and Sleep Quality in College Students: Cross-Sectional Study
Authors: Fildzah Badzlina, Mega Puspa Sari
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To rest the body after a full day of activities, the body needs sleep. During sleep, the body's response to external stimuli will be reduced and relatively inactive so that it is used to optimize the body's biological functions that cannot be done when awake. College students often experience poor sleep quality because of the dense activities carried out during the day. In addition, the level of physical activity of college students is also relatively low. Based on previous research, college students who have low physical activity have poor sleep quality. Therefore, the purpose of this study was to determine the relationship between physical activity and sleep quality in college students of the University of Muhammadiyah Prof. Dr. Hamka. This study used a cross-sectional research design with 107 respondents as research subjects. Samples were taken using the purposive sampling technique. The data was taken using a google form which was distributed to all college students in September 2021. The statistical test used was Chi-square. The results of this study showed that 85 (79.4%) college students experienced poor sleep quality during the Covid-19 Pandemic Period. Most respondents were 96 women (89.7%) and 32.7% (35 people) aged 20 years. In the pocket money category, most college students (71%) got pocket money less than 500.000 rupiahs per month. A total of 52 respondents (48.6%) had a moderate level of physical activity category. Poor sleep quality was more common in male students (90.9%) compared to female students (78.1%) (p>0.05). In the group with poor sleep quality, 88.9% of students were categorized in Rp. 500.001 to Rp. 1.000.000 for pocket money, 80.3% of students included in the category Rp. 500.000 or less, and 61.5% of students are included in the category of Rp. 1.000.000 or more. Poor sleep quality was more common among students in the age category 20 years (84.1%), compared to students in the age category > 20 years (71.1%). For the level of physical activity in the poor sleep quality group, 87% were included in the category of heavy physical activity, 82.7% included in the moderate level of physical activity, and 68.8% included in the category of low-level physical activity. There was no significant relationship between gender, pocket money, age, and physical activity with sleep quality (p>0.05).Keywords: college students, physical activity, sleep quality, university students
Procedia PDF Downloads 1406121 Phytochemical Screening and Evaluation of Antimicrobial and Antioxidant Activity of Anethum graveolens L. (Dill) Plant
Authors: Radhika S. Oke, Rebecca S. Thombre
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Medicinal plants and herbs have a great history of their utility as remedy for treatment of variety of ailments. Secondary metabolites present in these plants are responsible for their medicinal activity. In the present investigation, phytochemical screening of aqueous and alcoholic leaf extract of Anethum graveolens L. was performed. Total phenolic content and total antioxidant activity of the extracts was quantitatively estimated by Folin-Ciocalteau method and DPPH (1, 1-Diphenyl-2-picryl hydrazyl) method respectively. Qualitative tests suggested that Alkaloids, tannins and phenolic compounds were present in all the extracts of the plant. Aqueous extracts was found to have more phytochemicals as compared to alcoholic extracts. Extract of Anethum graveolens L. was found to contain good amount phenolics and exhibited antioxidant activity. The extracts also demonstrated potent antimicrobial activity against selected gram positive and negative bacteria. The study revealed the potential application of Anethum graveolens L. (Dill) in medicine and health.Keywords: Anethum graveolens L., antioxidant, antimicrobial activity, medicine and health
Procedia PDF Downloads 5066120 Local Activities of the Membranes Associated with Glycosaminoglycan-Chitosan Complexes in Bone Cells
Authors: Chih-Chang Yeh, Min-Fang Yang, Hsin-I Chang
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Chitosan is a cationic polysaccharide derived from the partial deacetylation of chitin. Hyaluronic acid (HA), chondroitin sulfate (CS) and heparin (HP) are anionic glycosaminoglycans (GCGs) which can regulate osteogenic activity. In this study, chitosan membranes were prepared by glutaraldehyde crosslinking reaction and then complexed with three different types of GCGs. 7F2 osteoblasts-like cells and macrophages Raw264.7 were used as models to study the influence of chitosan membranes on osteometabolism. Although chitosan membranes are highly hydrophilic, the membranes associated with GCG-chitosan complexes showed about 60-70% cell attachment. Furthermore, the membranes associated with HP-chitosan complexes could increase ALP activity in comparison with chitosan films only. Three types of the membranes associated with GCG-chitosan complexes could significantly inhibit LPS induced-nitric oxide expression. In addition, chitosan membranes associated with HP and HA can down-regulate tartrate-resistant acid phosphatase (TRAP) activity but not CS-chitosan complexes. Based on these results, we conclude that chitosan membranes associated with HP can increase ALP activity in osteoblasts and chitosan membranes associated with HP and HA reduce TRAP activity in osteoclasts.Keywords: osteoblast, osteoclast, chitosan, glycosaminoglycan
Procedia PDF Downloads 5276119 An Exploration of the Association Between the Physical Activity and Academic Performance in Internship Medical Students
Authors: Ali Ashraf, Ghazaleh Aghaee, Sedigheh Samimian, Mohaya Farzin
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Objectives: Previous studies have indicated the positive effect of physical activity and sports on different aspects of health, such as muscle endurance and sleep cycle. However, in university students, particularly medical students, who have limited time and a stressful lifestyle, there have been limited studies exploring this matter with proven statistical results. In this regard, this study aims to find out how regular physical activity can influence the academic performance of medical students during their internship period. Methods: This was a descriptive-analytical study. Overall, 160 medical students (including 80 women and 88 men) voluntarily participated in the study. The Baecke Physical Activity Questionnaire was applied to determine the student’s physical activity levels. The student's academic performance was determined based on their total average academic scores. The data were analyzed in SPSS version 16 software using the independent t-test, Pearson correlation, and linear regression. Results: The average age of the students was 26.0±1.5 years. Eighty-eight students (52.4%) were male, and 142 (84.5%) were single. The student's mean total average academic score was 16.2±1.2, and their average physical activity score was 8.3±1.1. The student's average academic score was not associated with their gender (P=0.427), marital status (P=0.645), and age (P=0.320). However, married students had a significantly lower physical activity level compared to single students (P=0.020). The results indicated a significant positive correlation between student's physical activity levels and average academic scores (r=+0.410 and P<0.001). This correlation was independent of the student’s age, gender, and marital status based on the regression analysis. Conclusion: The results of the current study suggested that the physical activity level in medical students was low to moderate in most cases, and there was a significant direct relationship between student’s physical activity level and academic performance, independent of age, gender, and marital status.Keywords: exercise, education, physical activity, academic performance
Procedia PDF Downloads 466118 Study of the in vivo and in vitro Antioxidant Activity of the Methanol Extract from the Roots of the Barks of Zizyphus lotus
Authors: Djemai Zoughlache Soumia, Yahia Mouloud, Lekbir Adel, Meslem Meriem, Maouchi Madiha, Bahi Ahlem, Benbia Souhila
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Natural extracts is known for their contents of biologically active molecules. In this context, we attempted to evaluate the antioxidant activity of the methanolic extract prepared from the bark of the roots of Zizyphus lotus. The quantitative analysis based on the dosage, phenolic compounds, flavonoids and tannins provided following values: 0.39 ± 0.007 ug EAG/mg of extract for phenolic compounds, 0.05 ± 0.02ug EQ/mg extract for flavonoids and 0.0025 ± 7.071 E-4 ECT ug/mg extract for tannins. The study of the antioxidant activity by the DPPH test in vitro showed a powerful antiradical power with an IC50 = 8,8 ug/ml. For the DPPH test in vivo we used two rats lots, one lot with a dose of 200 mg/kg of the methanol extract and a control lot. We found a significant difference in antiradical activity with p < 0.05.Keywords: Zizyphus lotus, antioxidant activity, DPPH, phenolic compounds, flavonoids, tannins
Procedia PDF Downloads 5096117 Antibacterial and Antioxidant Activities of Artemisia herba-alba Asso Essential Oil Growing in M’sila (Algeria)
Authors: Asma Meliani, S. Lakehal, F. Z. Benrebiha, C. Chaouia
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There is an increasing interest in phytochemicals as new source of natural antioxidant and antimicrobial agents. Plants essential oils have come more into the focus of phytomedicine. Many researchers have reported various biological and/or pharmacological properties of Artemisia herba alba Asso essential oil. The present study describes antimicrobial and antioxidant properties of Artemisia herba alba Asso essential oil. Artemisia herba alba Asso essential oil obtained by hydrodistillation (using Clevenger type apparatus) growing in Algeria (M’sila) was analyzed by GC-MS. The essential oil yield of the study was 0.7%. The major components were found to be camphor, chrysanthenone et 1,8-cineole. The antimicrobial activity of the essential oil was tested against four bacteria (Gram-negative and Gram-positive) and three fungi using the diffusion method and by determining the inhibition zone. The oil was found to have significant antibacterial activity. In addition, antioxidant activity was determined by 1, 1-diphenyl-1-picrylhydrazyl (DPPH) assay, ferric reducing (FRAP) assay and β-carotene bleaching test, and high activity was found for Artemisia herba-alba oil.Keywords: Artemisia herba-alba, essential oil, antibacterial activity, antioxidant activity
Procedia PDF Downloads 333