Search results for: biological activity

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

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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

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Authors: Parthiban Srinivasan

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With recent advances in computational power and access to enough data in biosciences, artificial intelligence methods are increasingly being used in drug discovery research. These methods are essentially a series of advanced statistics based exercises that review the past to indicate the likely future. Our goal is to develop a model that accurately predicts biological activity and toxicity parameters for novel compounds. We have compiled a robust library of over 150,000 chemical compounds with different pharmacological properties from literature and public domain databases. The compounds are stored in simplified molecular-input line-entry system (SMILES), a commonly used text encoding for organic molecules. We utilize an automated process to generate an array of numerical descriptors (features) for each molecule. Redundant and irrelevant descriptors are eliminated iteratively. Our prediction engine is based on a portfolio of machine learning algorithms. We found Random Forest algorithm to be a better choice for this analysis. We captured non-linear relationship in the data and formed a prediction model with reasonable accuracy by averaging across a large number of randomized decision trees. Our next step is to apply deep neural network (DNN) algorithm to predict the biological activity and toxicity properties. We expect the DNN algorithm to give better results and improve the accuracy of the prediction. This presentation will review all these prominent machine learning and deep learning methods, our implementation protocols and discuss these techniques for their usefulness in biomedical and health informatics.

Keywords: deep learning, drug discovery, health informatics, machine learning, toxicity prediction

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Authors: Tapiwa Brine Mutsauri

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The MEROPS system is an information resource for proteases that classifies them into clans according to their catalytic type. Within the Plant kingdom, cysteine ​​proteases are one of the best known, as they are the catalytic type on which the first studies on plant proteases were focused. Plant cysteine ​​proteases have a similar mechanism of action to serine proteases, and some are known to have activity on factors of the blood coagulation cascade, such as a potent antithrombotic effect, and also cause increased fibrinolysis. Of a few plant cysteine ​​proteases, the three-dimensional structure is known, so a method of interest to be able to predict their potential activity on the factors of the coagulation cascade would be to know their structure. Phylogenetics is the study of the evolutionary relationships between biological entities, often species, individuals, or genes (which can be called taxa). It is essential to identify the evolutionary position and the possible distribution of these enzymes in the plant kingdom, particularly those that act on coagulation factors. Bioinformatic tools, such as Clustal Omega / Jalview and Mega6, can be used to create phylogenetic trees. From the results of the alignment, it can be seen that although there is a certain degree of conservation (Conservation) and consensus (Consensus) among the eleven sequences, the functionally important motifs (those corresponding to the active site), the degree of conservation and consensus is very low. We could then infer that although activity on coagulation is reported for these enzymes, linked to their structural and mechanistic similarity with serine proteases, this activity may not have a direct or primary relationship with the proteolytic activity associated with their common, poorly conserved active site in this case. This ultimately could be related to modifications in the reaction mechanism of several of the enzymes studied, which would require more detailed study. Also, below, we will deal with factors that may have a greater influence on this result. The results of this work enrich the understanding of how species (and molecular sequences in general) evolve. Through phylogenetics, we learn not only how sequences came to be the way they are today but also the general principles that allow us to predict how they will change in the future. For pharmaceutical sciences, phylogenetic selection of biologically related species can help identify closely related members of a species with compounds of pharmacological importance, such as plant cysteine ​​proteases, in addition to identifying structural features that may influence their pharmacological activity and which can be valuable for drug design.

Keywords: computational simulation, proteases, coagulation, bioinformatics

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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

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Authors: Paweł Stączek, Tomasz Plech, Aleksandra Strzelczyk, Katarzyna Dzitko, Monika Wujec, Edyta Kuśmierz, Piotr Paneth, Agata Paneth

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In this contribution, we will describe the inhibitory potency of nine thiosemicarbazide derivatives against bacterial type IIA topoisomerases, their antibacterial profile, and molecular modeling evaluation. We have found that one of the tested compounds, 4-benzoyl-1-(2-methyl-furan-3-ylcarbonyl) thiosemicarbazide, remarkably inhibits the activity of S. aureus DNA gyrase with the IC50 below 5 μM. Besides, this compound displays antibacterial activity on Staphylococcus spp. and E. faecalis at non-cytotoxic concentrations in mammalian cells, with minimal inhibitory concentrations (MICs) values at 25 μg/mL. Based on the enzymatic and molecular modeling studies we propose two factors, i.e. geometry of molecule and hydrophobic/hydrophilic balance as important molecular properties for developing thiosemicarbazide derivatives as potent Staphylococcus aureus DNA gyrase inhibitors.

Keywords: bioactivity, drug design, topoisomerase, molecular modeling

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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

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Authors: Sanja O. Podunavac-Kuzmanović, Lidija R. Jevrić, Strahinja Z. Kovačević

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In last decade, metal-organic complexes have captured intensive attention because of their wide range of biological activities such as antibacterial, antifungal, anticancerous, antimicrobial and antiHIV. Therefore, it is of great importance for the development of coordination chemistry to explore the assembly of functional organic ligands with metal ion and to investigate the relationship between the structure and property. In view of our studies, we reasoned that benzimidazoles complexed to metal ions could act as a potent antibacterial agents. Thus, we have bioassayed the inhibitory potency of benzimidazoles and their metal salts (Co or Ni) against Gram negative bacteria Escherichia coli. In order to validate our in vitro study, we performed in silico studies using molecular docking software’s. The investigated compounds and their metal complexes (Co, Ni) showed good antibacterial activity against Escherichia coli. In silico docking studies of the synthesized compounds suggested that complexed benzimidazoles have a greater binding affinity and enhanced antibacterial activity in comparison with noncomplexed ligands. In view of their enhanced inhibitory properties we propose that the studied complexes can be used as potential pharmaceuticals. This study is financially supported by COST action CM1306 and the project No. 114-451-347/2015-02, financially supported by the Provincial Secretariat for Science and Technological Development of Vojvodina.

Keywords: benzimidazoles, complexes, antibacterial, Escherichia coli, metal

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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

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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

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Authors: Ghazi Bouaziz, Abderrahim Derouiche, Damien Brulin, Hélène Pigot, Eric Campo

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Automatic ADL classification is a crucial part of ambient assisted living technologies. It allows to monitor the daily life of the elderly and to detect any changes in their behavior that could be related to health problem. But detection of ADLs is a challenge, especially because each person has his/her own rhythm for performing them. Therefore, we used a correlation matrix to extract custom rules that enable to detect ADLs, including eating activity. Data collected from 3 different individuals between 35 and 105 days allows the extraction of personalized eating patterns. The comparison of the results of the process of eating activity extracted from the correlation matrices with the declarative data collected during the survey shows an accuracy of 90%.

Keywords: elderly monitoring, ADL identification, matrix correlation, meal-taking activity

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Authors: Fatma Zuhrotun Nisa, Aprilina Ratriany, Agus Wijanarka

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Background: Cassava leaves are widely used by the people of Indonesia as a vegetable and treat various diseases, including anticancer believed as food. However, not much research on the anticancer activity of cassava leaves, especially in colon cancer. Objectives: the aim of this study is to investigate anti-cancer activity of cassava leaves (Manihot esculanta C.) against colon cancer (WiDr) cells in vitro. Methods: effect of crude aqueous extract of leaves of cassava and cassava leaves boiled tested in colon cancer cells widr. Determination of Anticancer uses the MTT method with parameters such as the percentage of deaths. Results: raw cassava leaf water extract gave IC50 of 63.1 mg / ml. While the water extract of boiled cassava leaves gave IC50 of 79.4 mg/ml. However, there is no difference anticancer activity of raw cassava leaves or cancer (p> 0.05). Conclusion: Cassava leaves contain a variety of compounds that have previously been reported to have anticancer activity. Linamarin, β-carotene, vitamin C, and fiber were thought to affect the IC50 cassava leaf extract against colon cancer cells WiDr.

Keywords: boiled cassava leaves, cassava leaves raw, anticancer activity, colon cancer, IC50

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Authors: Malika Yaici, Soraya Aloui, Sara Semchaoui

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Recognition of human activities from sensor data is an active research area, and the main objective is to obtain a high recognition rate. In this work, we propose a recognition system based on expert systems. The proposed system makes the recognition based on the objects, object states, and gestures, taking into account the context (the location of the objects and of the person performing the activity, the duration of the elementary actions, and the activity). This work focuses on complex activities which are decomposed into simple easy to recognize activities. The proposed method can be applied to any type of activity. The simulation results show the robustness of our system and its speed of decision.

Keywords: human activity recognition, ubiquitous computing, context-awareness, expert system

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Authors: Thanawit Tongmai, Chatchawan Saewor

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Learning management is very important for students’ development. To promote students’ potential, the teacher should design appropriate learning activity that brings their students potential out. Problem based learning has been using worldwide and it has presented numerous of success. This research aims to study third year students’ attitude and their achievement in scientific research course. To find the results, mix method was used to design research conduction. The researcher used PBL and reflection activity in the class. The students had to choose a topic, reviewed information, designed experimental, wrote academic report and presented their research by themselves. The researcher was only a facilitator. Reflection activity was used to progressing and consulting their research. The data was collected along with research conduction by questionnaire and test, including attitude, opinion and their achievement. The result of this study showed that 74.71% from all of students (n = 87) benefited from PBL and reflection activity, while 25.19% were just satisfied. 100% of students had a positive reflection toward PBL activity and they believed that PBL was the best pedagogy method for scientific research course. The achievements of these students were higher than the previous study (P < 0.05). The student’s learning achievement, A, B+ and B, was 48.28, 28.74 and 22.98% respectively. Therefore, it can conclude that PBL activity is appropriate for scientific research course and it can also promote student’s achievement.

Keywords: reflection, attitude, learning, achievement, PBL

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Authors: Dana Craciun, Daniela Dascalu, Adriana Isvoran

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Phthalates are a class of plastic additives that are used to enhance the physical properties of plastics and as solvents in paintings and some of them proved to be of particular concern for the human health. There are insufficient data concerning the health risks of phthalates and further research on evaluating their effects in humans is needed. As humans are not volunteers for such experiments, computational analysis may be used to predict the biological effects of phthalates in humans. Within this study we have used some computational approaches (SwissADME, admetSAR, FAFDrugs) for predicting the absorption, distribution, metabolization, excretion and toxicity (ADME-Tox) profiles and pharmacokinetics for the most common used phthalates. These computational tools are based on quantitative structure-activity relationship modeling approach. The predictions are further compared to the known effects of each considered phthalate in humans and correlations between computational results and experimental data are discussed. Our data revealed that phthalates are a class of compounds reflecting high toxicity both when ingested and when inhaled, but by inhalation their toxicity is even greater. The predicted harmful effects of phthalates are: toxicity and irritations of the respiratory and gastrointestinal tracts, dyspnea, skin and eye irritations and disruption of the functions of liver and of the reproductive system. Many of investigated phthalates are predicted to be able to inhibit some of the cytochromes involved in the metabolism of numerous drugs and consequently to affect the efficiency of administrated treatments for many diseases and to intensify the adverse drugs reactions. The obtained predictions are in good agreement with clinical data concerning the observed effects of some phthalates in cases of acute exposures. Our study emphasizes the possible health effects of numerous phthalates and underlines the applicability of computational methods for predicting the biological effects of xenobiotics.

Keywords: phthalates, ADME-Tox, pharmacokinetics, biological effects

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Authors: Adesola Odole, Nse Odunaiya, Samuel Adewale

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Chronic Mechanical Low Back Pain (CMLBP) is prevalent in the aging population; some studies have documented the association among pain intensity, functional disability and physical activity in the general population but very few studies in the elderly. This study was designed to investigate the association among pain intensity, functional disability and physical activity of elderly individuals with CMLBP in the University College Hospital (UCH), Ibadan, Nigeria and also to determine the difference in physical activity, pain intensity and functional disability between males and females. A total of 96 participants diagnosed with CMLBP participated in this cross-sectional survey. They were conveniently sampled from selected units in the UCH, Ibadan, Nigeria. Data on sex, marital status, occupation and duration of onset of pain of participants were obtained from the participants. The Physical Activity Scale for the Elderly, Visual Analogue Scale and Oswestry Disability Questionnaire were used to measure the physical activity, pain intensity and functional disability of the participants respectively. Data was analysed using Spearman correlation, independent t-test; and α was set at 0.05. Participants (25 males, 71 females) were aged 69.64±7.43 years. The majority (76.0%) of the participants were married, and over half (55.2%) were retirees. Participants’ mean pain intensity score was 5.21±2.03 and mean duration of onset of low back pain was 63.63 ± 90.01 months. The majority (67.6%) of the participants reported severe to crippled functional disability. Their mean functional disability was 46.91 ± 13.99. Participants’ mean physical activity score was 97.47 ± 82.55. There was significant association between physical activity and pain intensity (r = -0.21, p = 0.04). There was significant association between physical activity and functional disability (r = -0.47, p = 0.00). Male (87.26 ± 79.94) and female (101.07 ± 83.71) participants did not differ significantly in physical activity (t = 0.00, p = 0.48). In addition, male (5.48 ± 2.06) and female (5.11 ± 2.02) participants’ pain intensity were comparable (t = 0.26, p = 0.44). There was also no significant difference in functional disability (t = 0.05, p = 0.07) between male (42.56 ±13.85) and female (48.45 ± 13.81) participants. It can be concluded from this study that majority of the elderly individuals with chronic mechanical low back pain had a severe to crippled functional disability. Those who reported increased physical activity had reduced pain intensity and functional disability. Male and female elderly individuals with chronic mechanical low back pain are comparable in their pain intensity, functional disability, and physical activity. Elderly individuals with CMLBP should be educated on the importance of participating in physical activity which could reduce their pain symptoms and improve functional disability.

Keywords: elderly, functional disability, mechanical low back pain, pain intensity, physical activity

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Authors: Mohamed E. Abdelrahamn, Mahmoud Aly Hassan, Mohamed Sarhan

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Subacromial impingement syndrome (SIS) is a common shoulder disorder. Patients often complain from a decrease in electromyography (EMG) activity of the rotator cuff muscles especially the supraspinatus muscle during glenohumeral elevation. Objective: The purpose of the study is to assess the effect of applying 50% of maximum voluntary contraction of hand grip strength on the EMG activity of the shoulder muscles in patients with SIS. Methods: Thirty male and female patients participated in this study. Their ages ranged from 25 to 40 years. EMG activity of supraspinatus muscle and middle deltoid muscle was assessed without and with applying 50% of maximum voluntary contraction (MVC). Results: A significant difference was found for both supraspinatus and middle deltoid muscles, indicating that the gripping resulted in increasing muscle activity. Conclusion: Applying 50% MVC of hand grip strength could increase the supraspinatus and middle deltoid muscles activity in patients of SIS. This might be useful in the development and monitoring of shoulder rehabilitation strategies.

Keywords: electromyography, supraspinatus muscle, deltoid muscle, subacromial impingement syndrome

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Authors: Reem I. Altamimi, Geoff D. Skinner

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Extended periods engaged in sedentary behavior increases the risk of becoming overweight and/or obese which is linked to other health problems. Adding technology to the term ‘active living’ permits its inclusion in promoting and facilitating habitual physical activity. Technology can either act as a barrier to, or facilitate this lifestyle, depending on the chosen technology. Physical Activity Monitoring Technologies (PAMTs) are a popular example of such technologies. Different contemporary PAMTs have been evaluated based on customer reviews; however, there is a lack of published experimental research into the efficacy of PAMTs. This research aims to investigate the reliability of four PAMTs: two wristbands (Fitbit Flex and Jawbone UP), a waist-clip (Fitbit One), and a mobile application (iPhone Health Application) for recording a specific distance walked on a treadmill (1.5km) at constant speed. Physical activity tracking technologies are varied in their recordings, even while performing the same activity. This research demonstrates that Jawbone UP band recorded the most accurate distance compared to Fitbit One, Fitbit Flex, and iPhone Health Application.

Keywords: Fitbit, jawbone up, mobile tracking applications, physical activity tracking technologies

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Authors: Yong Geun Yun, Jong Hui kim, Sang Ho Baik

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This study was carried out to develop a fermented dandelion (Tarazacum officinale) beverage using lactic acid bacteria with cinnamoyl esterase (CE) activity isolated from human feces. Lactic acid bacteria were screened based on bacterial survival ability in dandelion extract and CE activity. Dandelion extract fermented by Lactobacillus acidophilus F-46 (LA-F46) maintained approximately 105-106 log CFU/mL over an 8 days period. After fermented dandelion beverage (FDB) with LA-46 for 8 days at 37oC the pH was decreased from pH 7.0 to 3.5. Antioxidant activity by using DPPH radical scavenging activity of the prepared FDB was significantly increased compared to that of non-fermented dandelion beverage (NFDB). Moreover, CE activity was significantly enhanced during fermentation and showed the approximately 4.3 times increased concentration of caffeic acid up to 9.91 mg/100 mL after 8 days of incubation compared to NFDB. Therefore, it concluded that dandelion can be a good source for preparing a functional beverage and fermentation by LA-F46 enhanced the food functionality with enhanced caffeic acids.

Keywords: cinnamoyl esterase, dandelion, fermented beverage, lactic acid bacteria

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Authors: Mohamed M. Bumadian, D. James Gilmour

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Three bacterial species were isolated from the River Wye (Derbyshire, England) and identified using 16S rRNA gene sequencing as Serratia proteamaculans, Aeromonas hydrophila and Klebsiella pneumoniae. Respiration rates of the strains were measured in order to determine the metabolic activity under salt stress. The highest respiration rates of all three strains were found at 0.17 M and 0.5 M NaCl and then the respiration rate decreased with increasing concentrations of NaCl. In addition, the effect of increasing concentrations of NaCl on malate dehydrogenase activity was determined using cell-free extracts of the three strains. Malate dehydrogenase activity was stimulated at NaCl concentrations up to 0.5 M, and a small level of activity remained even at 3.5 M NaCl. The pH optimum of the malate dehydrogenase in cell-free extracts of all strains was higher than pH 7.5.

Keywords: fresh water, halotolerant pathogenic bacteria, 16S rRNA gene, cell-free extracts, respiration rates, malate dehydrogenase

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Authors: Stefan Gruden, Charlott Brunmark, Bo Holmqvist, Erwin D. Brenndorfer, Martin Johansson, Jian Liu, Ying Zhao, Niklas Axen, Moustapha Hassan

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Aim: The study was designed to evaluate the ability of the calcium sulfate-based NanoZolid® drug delivery technology to locally release the epidermal growth factor (EGF) protein while maintaining its biological activity. Methods: NanoZolid-formulated EGF protein labelled with a near-infrared dye (EGF-NIR) depots or EGF-NIR dissolved in PBS were injected subcutaneously into mice bearing EGF receptor (EGFR) positive human A549 lung cancer tumors inoculated subcutaneously. The release and biodistribution of the EGF-NIR were investigated in vivo longitudinally up to 96 hours post-administration, utilizing whole-body fluorescence imaging. In order to confirm the in vivo findings, histological analysis of tumor cryosections was performed to investigate EGF-NIR fluorescent signal and EGFR expression level by immunofluorescence labelling. Results: The in vivo fluorescence imaging showed a controlled release profile of the EGF-NIR loaded in the NanoZolid depots compared to free EGF-NIR. Histological analysis of the tumors further demonstrated a prevailing distribution of EGF-NIR in regions with high levels of EGFR expression. Conclusion: Calcium sulfate based depots can be used to formulate EGF while maintaining its biological activity, e.g., receptor binding capability. This may have good clinical potential for local delivery of biomolecules to enhance treatment efficacy and minimize systemic adverse effects.

Keywords: bioresorbable, calcium sulfate, controlled release, NanoZolid

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Authors: I. Tulay Cagatay

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Blue-green microalgae cyanobacteria, which are important photosynthetic organisms of aquatic ecosystems, are the primary sources of many bioactive compounds such as proteins, carbohydrates, lipids, vitamins and enzymes that can be used as antimicrobial and antiviral agents. Some of these organisms are nowadays used directly in the food, cosmetic and pharmaceutical industry, or in aquaculture and biotechnological approaches like biofuel or drug therapy. Finding the effective, environmental friendly chemotropic and antimicrobial agents to control fish pathogens are crucial in a country like Turkey which has a production capacity of about 240 thousand tons of cultured fish and has 2377 production farms and which is the second biggest producer in Europe. In our study, we tested the antimicrobial activity of cyanobacterium spp. against some fish pathogens Aeromonas hydrophila and Yersinia ruckeri that are important pathogens for rainbow trout farms. Agar disk diffusion test method was used for studying antimicrobial activity on pathogens. Both tested microorganisms have shown antimicrobial activity positively as the inhibition zones were 0.45 mm and 0.40 mm respectively.

Keywords: fish pathogen, cyanobacteria, antimicrobial activity, trout

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Authors: T. Ould Bellahcen, A. Amiri, I. Touam, F. Hmimid, A. El Amrani, M. Cherki

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The antioxidant activity of three extracts (water, lipidic and ethanolic) prepared from the microalgae Spirulina platensis isolated from Moroccan lake, using 2, 2 diphenyl-1-picrylhydrazyl (DPPH) and 2,2’-azino-bis ethylbenzthiazoline-6-sulfonic acid (ABTS) radical assay, was studied and compared. The obtained results revealed that the IC₅₀ found using DPPH were lower than that of ABTS for all extracts from these planktonic blue-green algae. The high levels of phenolic and flavonoid content were found in the ethanolic extract 0,33 ± 0,01 mg GAE/g dw and 0,21 ± 0,01 mg quercetin/g dw respectively. In addition, using DPPH, the highest activity with IC₅₀ = 0,449 ± 0,083 mg/ml, was found for the ethanolic extract, followed by that of lipidic extract (IC₅₀ = 0,491 ± 0,059 mg/ml). The lowest activity was for the aqueous extract (IC₅₀ = 4,148 ± 0,132 mg/ml). For ABTS, the highest activity was observed for the lipidic extract with IC₅₀ = 0,740 ± 0,012 mg/ml, while, the aqueous extract recorded the lowest activity (IC₅₀ = 6,914 ± 0, 0067 mg/ml). A moderate activity was showed for the ethanolic extract (IC₅₀ = 5,852 ± 0, 0171 mg/ml). It can be concluded from this first study that Spirulina platensis extracts show an interesting antioxidant and antiradicals properties suggesting that this alga could be used as a potential source of antioxidants. A qualitative and quantitative analysis of polyphenol and flavonoids in the extracts using HPLC is in progress so as to study the correlation between the antioxidant activity and chemical composition.

Keywords: Spirulina platensis, antioxidant, DPPH, ABTS

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Authors: Manohar Salla, Mark S. Butler, Ruby Pelingon, Geraldine Kaeslin, Daniel E. Croker, Janet C. Reid, Jong Min Baek, Paul V. Bernhardt, Elizabeth M. J. Gillam, Matthew A. Cooper, Avril A. B. Robertson

Abstract:

MCC950 is a potent and selective inhibitor of the NOD-like receptor pyrin domain-containing protein 3 (NLRP3) inflammasome that shows early promise for treatment of inflammatory diseases. The identification of major metabolites of lead molecule is an important step during drug development process. It provides an information about the metabolically labile sites in the molecule and thereby helping medicinal chemists to design metabolically stable molecules. To identify major metabolites of MCC950, the compound was incubated with human liver microsomes and subsequent analysis by (+)- and (−)-QTOF-ESI-MS/MS revealed a major metabolite formed due to hydroxylation on 1,2,3,5,6,7-hexahydro-s-indacene moiety of MCC950. This major metabolite can lose two water molecules and three possible regioisomers were synthesized. Co-elution of major metabolite with each of the synthesized compounds using HPLC-ESI-SRM-MS/MS revealed the structure of the metabolite (±) N-((1-hydroxy-1,2,3,5,6,7-hexahydro-s-indacen-4-yl)carbamoyl)-4-(2-hydroxypropan-2-yl)furan-2-sulfonamide. Subsequent synthesis of individual enantiomers and coelution in HPLC-ESI-SRM-MS/MS using a chiral column revealed the metabolite was R-(+)- N-((1-hydroxy-1,2,3,5,6,7-hexahydro-s-indacen-4-yl)carbamoyl)-4-(2-hydroxypropan-2-yl)furan-2-sulfonamide. To study the possible cytochrome P450 enzyme(s) responsible for the formation of major metabolite, MCC950 was incubated with a panel of cytochrome P450 enzymes. The result indicated that CYP1A2, CYP2A6, CYP2B6, CYP2C9, CYP2C18, CYP2C19, CYP2J2 and CYP3A4 are most likely responsible for the formation of the major metabolite. The biological activity of the major metabolite and the other synthesized regioisomers was also investigated by screening for for NLRP3 inflammasome inhibitory activity and cytotoxicity. The major metabolite had 170-fold less inhibitory activity (IC50-1238 nM) than MCC950 (IC50-7.5 nM). Interestingly, one regioisomer had shown nanomolar inhibitory activity (IC50-232 nM). However, no evidence of cytotoxicity was observed with any of these synthesized compounds when tested in human embryonic kidney 293 cells (HEK293) and human liver hepatocellular carcinoma G2 cells (HepG2). These key findings give an insight into the SAR of the hexahydroindacene moiety of MCC950 and reveal a metabolic soft spot which could be blocked by chemical modification.

Keywords: Cytochrome P450, inflammasome, MCC950, metabolite, microsome, NLRP3

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Authors: Kyungae Jo, Eun Young Kim, Byungsoo Shin, Kwang Soon Shin, Hyung Joo Suh

Abstract:

Gamma-aminobutyric acid (GABA) and 5-hydroxytryptophan (5-HTP) are amino acids of digested nutrients or food ingredients and these can possibly be utilized as non-pharmacologic treatment for sleep disorder. We previously investigated the GABA/5-HTP mixture is the principal concept of sleep-promoting and activity-repressing management in nervous system of D. melanogaster. Two experiments in this study were designed to evaluate sleep-promoting effect of GABA/5-HTP mixture, to clarify the possible ratio of sleep-promoting action in the Drosophila invertebrate model system. Behavioral assays were applied to investigate distance traveled, velocity, movement, mobility, turn angle, angular velocity and meander of two amino acids and GABA/5-HTP mixture with caffeine treated flies. In addition, differentially expressed gene (DEG) analyses from next generation sequencing (NGS) were applied to investigate the signaling pathway and functional interaction network of GABA/5-HTP mixture administration. GABA/5-HTP mixture resulted in significant differences between groups related to behavior (p < 0.01) and significantly induced locomotor activity in the awake model (p < 0.05). As a result of the sequencing, the molecular function of various genes has relationship with motor activity and biological regulation. These results showed that GABA/5-HTP mixture administration significantly involved the inhibition of motor behavior. In this regard, we successfully demonstrated that using a GABA/5-HTP mixture modulates locomotor activity to a greater extent than single administration of each amino acid, and that this modulation occurs via the neuronal system, neurotransmitter release cycle and transmission across chemical synapses.

Keywords: sleep, γ-aminobutyric acid, 5-hydroxytryptophan, Drosophila melanogaster

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Authors: Emma O’ Keeffe, Helen Hughes, Peter McLoughlin, Shiau Pin Tan, Nick McCarthy

Abstract:

Biosecurity is emerging as one of the most important issues facing the agricultural and forestry community. This is as a result of increased invasion from new pests and diseases with the main protocol for dealing with these species being the use of synthetic pesticides. However, these chemicals have been shown to exhibit negative effects on the environment. Seaweeds represent a vast untapped resource of bio-molecules with a broad range of biological activities including pesticidal. This project investigated both the antifungal and antibacterial activity of seaweed species against two problematic root rot fungi, Armillaria mellea and Heterobasidion annosum and ten quarantine bacterial plant pathogens including Xanthomonas arboricola, Xanthomonas fragariae, and Erwinia amylovora. Four seaweed species were harvested from the South-East coast of Ireland including brown, red and green varieties. The powdered seaweeds were extracted using four different solvents by liquid extraction. The poisoned food technique was employed to establish the antifungal efficacy, and the standard disc diffusion assay was used to assess the antibacterial properties of the seaweed extracts. It was found that extracts of the green seaweed exhibited antifungal activity against H. annosum, with approximately 50% inhibition compared to the negative control. The protectant activities of the active extracts were evaluated on disks of Picea sitchensis, a plant species sensitive to infection from H. annosum and compared to the standard chemical control product urea. The crude extracts exhibited very similar activity to the 10% and 20% w/v concentrations of urea, demonstrating the ability of seaweed extracts to compete with commercially available products. Antibacterial activity was exhibited by a number of seaweed extracts with the red seaweed illustrating the strongest activity, with a zone of inhibition of 15.83 ± 0.41 mm exhibited against X. arboricola whilst the positive control (10 μg/disk of chloramphenicol) had a zone of 26.5 ± 0.71 mm. These results highlight the potential application of seaweed extracts in the forestry and agricultural industries for use as biopesticides. Further work is now required to identify the bioactive molecules that are responsible for this antifungal and antibacterial activity in the seaweed extracts, including toxicity studies to ensure the extracts are non-toxic to plants and humans.

Keywords: antibacterial, antifungal, biopesticides, seaweeds

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Authors: M. P. Casiraghi, C. M. Quintella, P. Almeida

Abstract:

Paraffinic oils were submitted to microbial action. The microorganisms consisted of bacteria of the genera Pseudomonas sp and Bacillus lincheniforms. The alterations in interfacial tension were determined using a tensometer and applying the hanging drop technique at room temperature (299 K ±275 K). The alteration in the constitution of the paraffins was evaluated by means of gas chromatography. The microbial activity was observed to reduce interfacial tension by 54 to 78%, as well as consuming the paraffins C19 to C29 and producing paraffins C36 to C44. The LIFirr technique made it possible to determine the microbial action quickly.

Keywords: paraffins, biosurfactants, LIFirr, microbial activity

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Authors: Randa M. T. Mohamed

Abstract:

Spices have long been used as traditional ingredients in the kitchen for seasoning, coloring, aromatic and food preservative properties. Besides, spices are equally used for therapeutic purposes. The objective of this study was to survey and document the medicinal properties of spices commonly used in the Sudanese kitchen for different food preparations. Also, extracts from reported spices were screened for the presence of secondary metabolites as well as their antioxidant and beta-lactamase inhibitory properties. This study was conducted in the Rekabbya Quartier in Omdurman, Khartoum State, Sudan. Information was collected by carrying out semi-structured interviews. All informants (30) in the present study were women. Spices were purchased from Attareen shop in Omdurman. Essential oils from spices were extracted by hydrodistillation, and ethanolic extracts by maceration. Phytochemical screening was performed by thin-layer chromatography (TLC). The antioxidant capacity of essential oils and ethanolic extracts was investigated through TLC bioautography. Beta lactamase inhibitory activity was performed by the acidimetric test. Ethnobotany study showed that a total of 16 spices were found to treat 36 ailments belonging to 10 categories. The most frequently claimed medicinal uses were for the digestive system diseases treated by 14 spices and respiratory system diseases treated by 8 spices. Gynecological problems were treated with 4 spices. Dermatological diseases were cured by 5 spices, while infections caused by tapeworms and other microbes causing dysentery were treated by 3 spices. 4 spices were used to treat bad breath, bleeding gum and toothache. Headache, eyes infection, cardiac stimulation and epilepsy were treated with one spice each. Other health problems like fatigue and loss of appetite, and low breast milk production were treated by 1, 3 and 2 spices, respectively. The majority (69%, 11/16) of spices were exported from different countries like India, China, Indonesia, Ethiopia, Egypt and Nigeria, while 31% (5/16) was cultivated in Sudan. Essential oils of all spices were rich in terpenes, while ethanolic extracts contained variable classes of secondary metabolites. Both essential oils and ethanolic extracts of all spices exerted considerable antioxidant activity. Only one extract, Syzygium aromaticum, possessed beta-lactamase inhibitory activity. In conclusion, this study could contribute to conserving information on traditional medicinal uses of spices in Sudan. Also, the results demonstrated the potential of some of these spices to exert beneficial antimicrobial and antioxidant effects. Detailed phytochemical and biological assays of these spices are recommended.

Keywords: spices, enthnobotany, antioxidant, betalactamase inhibition

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Authors: Amel Benhadji, Mourad Taleb Ahmed, Rachida Maachi

Abstract:

The challenge for the new millennium is to develop an industrial system that has minimal socio-ecological impacts, without compromising quality of life. Leather industry is one of these industries demanding environmentally friendly products. In this study, we investigated the possibility of applying innovative low cost biological treatment using Pseudomonas aeruginosa. This strain tested the efficiency of the batch biological treatment in the recovery of protein and hexavalent chromium from chromium tanning bath. We have compared suspended and fixed bacteria culture. The results showed the removal of the total protein of treatment and a decrease of hexavalent chromium concentration is during the treatment. The better efficiency of the biological treatment is obtained when using fixed culture of P. aeruginosa.

Keywords: tanning wastewater, biological treatment, protein removal, hexavalent chromium

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Authors: N. Saki, S. Nalbantoglu, M. Akin, G. Arabaci

Abstract:

Walnut has a great range of phenolic profile and it is used in Asia and Africa for treatment of many diseases and cancer. Phenolic compounds play a number of crucial roles in complex metabolism of plants and of also fruit trees. Consumption of certain phenolics in the food is considered beneficial for human nutrition. Phenolic compounds known as anti-radical inactivators with their high antioxidant activities and these activities play an important role in inhibition of multi-metal corrosion. Many common corrosion inhibitors that are still in use today are health hazards. Therefore, there is still an increased attention directed towards the development of environmentally compatible, nonpolluting corrosion inhibitors. The present study reports the total phenols content, antioxidant potentials and tyrosinase inhibitory activity of the walnut (Juglans regia L.) produced in Turkey. The anti-tyrosinase activity was investigated for walnut at 2 h extraction time and all extracts exhibited tyrosinase activity. The results of this study suggested that walnut can be used as an excellent, easily accessible source of natural antioxidant.

Keywords: antioxidant activity, Juglans Regia, total phenols, tyrosinase activity

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