Search results for: cytotoxic activity
5943 Quantitative Structure-Activity Relationship Analysis of Binding Affinity of a Series of Anti-Prion Compounds to Human Prion Protein
Authors: Strahinja Kovačević, Sanja Podunavac-Kuzmanović, Lidija Jevrić, Milica Karadžić
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The present study is based on the quantitative structure-activity relationship (QSAR) analysis of eighteen compounds with anti-prion activity. The structures and anti-prion activities (expressed in response units, RU%) of the analyzed compounds are taken from CHEMBL database. In the first step of analysis 85 molecular descriptors were calculated and based on them the hierarchical cluster analysis (HCA) and principal component analysis (PCA) were carried out in order to detect potential significant similarities or dissimilarities among the studied compounds. The calculated molecular descriptors were physicochemical, lipophilicity and ADMET (absorption, distribution, metabolism, excretion and toxicity) descriptors. The first stage of the QSAR analysis was simple linear regression modeling. It resulted in one acceptable model that correlates Henry's law constant with RU% units. The obtained 2D-QSAR model was validated by cross-validation as an internal validation method. The validation procedure confirmed the model’s quality and therefore it can be used for prediction of anti-prion activity. The next stage of the analysis of anti-prion activity will include 3D-QSAR and molecular docking approaches in order to select the most promising compounds in treatment of prion diseases. These results are the part of the project No. 114-451-268/2016-02 financially supported by the Provincial Secretariat for Science and Technological Development of AP Vojvodina.Keywords: anti-prion activity, chemometrics, molecular modeling, QSAR
Procedia PDF Downloads 3045942 Risk of Occupational Exposure to Cytotoxic Drugs: The Role of Handling Procedures of Hospital Workers
Authors: J. Silva, P. Arezes, R. Schierl, N. Costa
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In order to study environmental contamination by cytostatic drugs in Portugal hospitals, sampling campaigns were conducted in three hospitals in 2015 (112 samples). Platinum containing drugs and fluorouracil were chosen because both were administered in high amounts. The detection limit was 0.01 pg/cm² for platinum and 0.1 pg/cm² for fluorouracil. The results show that spills occur mainly on the patient`s chair, while the most referenced occurrence is due to an inadequately closed wrapper. Day hospitals facilities were detected as having the largest number of contaminated samples and with higher levels of contamination.Keywords: cytostatic, contamination, hospital, procedures, handling
Procedia PDF Downloads 2955941 Clove Essential Oil Improves Lipid Peroxidation and Antioxidant Activity in Tilapia Fish Fillet Cooked by Grilling and Microwaving
Authors: E. Oskoueian, E. Maroufyan, Y. M. Goh, E. Ramezani-Fard, M. Ebrahimi
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The fish meat plays an important role in the human health as it contains high quality protein. The tilapia fish considered as the third largest group of farmed fish. The oxidative deterioration of fish meat may occur during the cooking process. The proper cooking process and using natural antioxidant to prevent oxidation and enhance the quality of the tilapia fish fillet is necessary. Hence, this research was carried out to evaluate the potential of clove essential oil to prevent lipid peroxidation and enhance the antioxidant activity of tilapia fish fillet cooked using microwave and griller. The results showed that cooking using microwave significantly (p < 0.05) increased the lipid peroxidation and decreased the DPPH and ferric reducing activity power of the fish fillet as compared to grilling. The fortification of fish fillet using clove essential oil prevented from lipid peroxidation and enhanced the antioxidant activity of the fish fillet significantly (p < 0.05). Consequently, fortification of tilapia fish fillet using clove essential oil followed by cooking using griller to have high quality cooked fish meat is recommended.Keywords: antioxidant activity, fillet, fish, fortification, lipid peroxidation
Procedia PDF Downloads 4545940 Antioxidant Activity of Selected Medicinal Plants Used in Folk Medicine in Libya
Authors: Salmin Alshalmani, Ghazall M Benhusein, Ebtisam Alhadi Absomaha, Marwa I. Meshri, Hamdoon A. Mohammed, Jamal Mezogi
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Eight wild medicinal plants used by Libyan and growing in Al-Jebel Al-Akhdar, Libya were suspected to estimate the antioxidant activity using 2,2-Diphenyl-1-Picrylhydrazyl stable free radical (DPPH). Incidences of purple colour reduction of the DPPH by testing extracts in addition to quercetin and vitamin C as positive controls reflect its ability to scavenge free radicals. All testing plants extract showed noticeable strength as antioxidant regarding its abilities to scavenge DPPH with an especial regards to Sarcopoterium spinosum.Keywords: antioxidant, scavenging activity, folk medicine, methanol extracts
Procedia PDF Downloads 6015939 The Importance of Conserving Pre-Historical, Historical and Cultural Heritage and Its Tourist Exploitation
Authors: Diego Renan G. Tudela, Veruska C. Dutra, Mary Lucia Gomes Silveira de Senna, Afonso R. Aquino
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Tourism in the present is the largest industry in the world, being an important global activity that has grown a lot in recent times. In this context, the activity of cultural tourism is growing, being seen as an important source of knowledge and information enjoyed by visitors. This article aims to discuss the cultural tourism, archaeological records and indigenous communities and the importance of preserving these invaluable sources of information, focusing on the records of the first peoples inhabiting the South American and North American lands. The study was based on discussions, theoretical studies, bibliographical research. Archaeological records are an important source of knowledge and information. Indigenous ethnic tourism represents a rescue of the authenticity of indigenous traditional cultures and their relation to the natural habitat. Cultural and indigenous tourism activity requires long-term planning to make it a sustainable activity.Keywords: tourism, culture, preservation, discussions
Procedia PDF Downloads 2625938 Antibacterial Activity of Trans-Cinnamaldehyde and Geraniol and Their Potential as Ingredients of Biocidal Polymers
Authors: Daria Olkiewicz, Maciej Walczak
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In this paper, the biocidal effects of trans-cinnamaldehyde (a main component of cinnamon oil) and geraniol (a constituent of Pelargonium graveolens essential oil) are presented. The activity of the combination of trans-cinnamaldehyde and geraniol was tested against 3 bacterial strains: Staphylococcus aureus ATCC6538 (Gramm+), Escherichia coli ATCC8739 (Gramm-, Lac+) and Pseudomonas aeruginosa KKP 991(Gramm-, Lac-). The biocidal activity of trans-cinnamaldehyde-geraniol mixture against bacteria mentioned above was evaluated by disk-diffusion method. The model strains were exposed on 1, 2.5, 5 and 10 mg of trans-cinnamaldehyde-geraniol mixture per disk, and all strains were susceptible to this combination of plant compounds. For all microorganisms, also Minimal Inhibitory Concentration (MIC) and Minimal Bactericidal Concentration (MBC) were estimated. For Staphylococcus aureus MIC was 0.0625 mg/ml of the trans-cinnamaldehyde and geraniol mixture, and MBC was 1.25 mg/ml; For Escherichia coli MIC=0.5 mg/ml, MBC=1 mg/ml, and finally Pseudomonas aeruginosa was inhibited in 0.5 mg/ml, and minimal biocidal concentration of tested mixture for it was 1.25 mg/ml. There are also reports about the synergistic working of trans-cinnamaldehyde and geraniol against microorganisms and the antimicrobial activity of polymers enriched with trans-cinnamaldehyde or geraniol, therefore the successful development and introduction to the today life of biocidal polymer enriched with trans-cinnamaldehyde and geraniol are possible.Keywords: antibacterial activity, biocidal polymers, geraniol, trans-cinnamaldehyde
Procedia PDF Downloads 1785937 Essential Oil Composition and Antimicrobial Activity of Rosmarinus officinalis L. Grown in Algeria (Djelfa)
Authors: Samah Lakehal, A. Meliani, F. Z. Benrebiha, C. Chaouia
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In the last few years, due to the misuse of antibiotics and an increasing incidence of immunodeficiency-related diseases, the development of microbial drug resistance has become more and more of a pressing problem. Recently, natural products from medicinal plants represent a fertile ground for the development of novel antibacterial agents. Plants essential oils have come more into the focus of phytomedicine. The present study describes antimicrobial activity of Rosmarinus officinalis L. essential oil known medicinally for its powerful antibacterial properties. The essential oil of rosemary obtained by hydrodistillation (using Clevenger type apparatus) growing in Algeria (Djelfa city of south Algeria) was investigated by GC-MS. The essential oil yield of the study was 1.4 %. The major components were found to be camphor, camphene, 1,8-cineole. The essential oil has been tested for antimicrobial activity against eight bacteria (Gram-negative and Gram-positive), and three fungi including Candida albicans. Inhibition of growth was tested by the agar diffusion method based on the determination of the diameter of inhibition. The oil was found to have significant antibacterial activity and therefore can be used as a natural antimicrobial agent for the treatment of several infectious diseases caused by those germs, which have developed resistance to antibiotics.Keywords: antimicrobial activity, Rosmarinus officinalis L., essential oils, GC/MS, camphor
Procedia PDF Downloads 3925936 The Term Spread Impact on Economic Activity for Transition Economies: Case of Georgia
Authors: L. Totladze
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The role of financial sector in supporting economic growth and development is well acknowledged. The term spread (the difference between the yields on long-term and short-term Treasury securities) has been found useful for predicting economic variables as output growth, inflation, industrial production, consumption. The temp spread is one of the leading economic indicators according to NBER methodology. Leading economic indicators are widely used in forecasting of economic activity. Many empirical studies find that the term spread predicts future economic activity. The article shortly explains how the term spread might predict future economic activity. This paper analyses the dynamics of the spread between short and long-term interest rates in countries with transition economies. The research paper analyses term spread dynamics in Georgia and compare it with post-communist countries and transition economies spread dynamics. In Georgia, the banking sector plays an important and dominant role in the financial sector, especially with respect to the mobilization of savings and provision of credit and may impact on economic activity. For this purpose, we study the impact of the term spread on economic growth in Georgia.Keywords: forecasting, leading economic indicators, term spread, transition economies
Procedia PDF Downloads 1765935 Free Raducal Scavenging Activity of Fractionated Extract and Structural Elucidation of Isolated Compounds from Hydrocotyl Bonariensis Comm. Ex Lam Leaves
Authors: Emmanuel O Ajani, Sabiu S, Mariam Zakari, Fisayo A Bamisaye
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Hydrocotyl bonariensis is a plant which anticataractogenic potentials have been reported. In the present study an attempt was made to evaluate the in vitro antioxidant activity of the fractionates of the leaves extract and also characterize some of its chemical constituents. DPPH, H₂O₂, OH and NO free radical scavenging, metal chelating and reducing power activity was used to evaluate the antioxidant activity of the crude extract fractionates. Fresh leaves of Hydrocotyl bonariensis leaves were extracted in 70% methanol. The extract was partitioned with different solvent system of increasing polarity (n-hexane, chloroform, ethyl acetate methanol and water). Compounds were isolated from the aqueous practitionate using accelerated gradient chromatography, vacuum liquid chromatography, preparative TLC and conventional column chromatography. The presence of the chemical groups was established with HPLC and Fourier Transform Infra Red. The structures of isolated compounds were elucidated by spectroscopic study and chemical shifts. Data from the study indicates that all the fractionates contain compounds with free radical scavenging activity. This activity was more pronounced in the aqueous fractionate (DPPH IC₅₀, 0025 ± 0.011 mg/ml, metal chelating capacity 27.5%, OH- scavenging IC₅₀, 0.846 ± 0.037 mg/ml, H₂O₂ scavenging IC₅₀ 0.521 ± 0.015 mg/ml, reducing power IC₅₀ 0.248 ± 0.025 mg/ml and NO scavenging IC₅₀ 0.537 ± 0.038 mg/ml). Two compounds were isolated and when compared with data from the literature; the structures were suggestive of polyphenolic flavonoid, quercetin and 3-O-β-D-glucopyranosyl-sitosterol. The result indicates that H. bonariensis leaves contain bioactive compounds with antioxidant activity.Keywords: antioxidant, cataract, free radical, flavonoids, hydrocotyl bonariensis
Procedia PDF Downloads 2705934 Physical Activity Levels in Qatar: A Pedometer-Based Assessment
Authors: Suzan Sayegh, Izzeldin Ibrahim, Mercia Van Der Walt, Mohamed Al-Kuwari
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Background: Walking is the most common form of physical activity which can promote a healthy well-being among people of different age groups. In this regard, pedometers are becoming more popular within research and are considered useful tools in monitoring physical activity levels based on individuals’ daily steps. A value of ˂5,000 steps/day is identified as a sedentary lifestyle index where individuals are physically inactive. Those achieving 5,000-7,499 steps/day have a low active lifestyle as they do not meet the moderate-to-vigorous physical activity (MVPA) recommendations. Moreover, individuals achieving ≥7,500 steps/day are classified as physically active. The objective of this study is to assess the physical activity levels of adult population in Qatar through a pedometer-based program over a one-year period. Methods: A cross-sectional analysis, as part of a longitudinal study, was carried out over one year to assess the daily step count. “Step into Health” is a community-based program launched by Aspire as an approach for the purpose of improving physical activity across the population of Qatar. The program involves distribution of pedometers to registered members which is supported by a self-monitoring online account and linked to a web database. Daily habitual physical activity (daily total step count) was assessed through Omron HJ-324U pedometer. Analyses were done on data extracted from the web database. Results: A total of 1,988 members were included in this study (males: n=1,143, 57%; females: n=845, 43%). Average age was 37.8±10.9 years distributed as 60% of age between age 25-54 (n=1,186), 27% of age 45-64 (n=546), and 13% of age 18-24 years (n=256). Majority were non-Qataris, 81% (n=1,609) compared with 19% of the Qatari nationality (n=379). Average body mass index (BMI) was 27.8±6.1 (kg/m2) where most of them (41%, n=809) were found to be overweight, between 25-30 kg/m2. Total average step count was 5,469±3,884. Majority were found to be sedentary (n=1110, 55.8%). Middle aged individuals were more active than the other two age groups. Males were seen as more active than females. Those who were less active had a higher BMI. Older individuals were more active. There was a variation in the physical activity level throughout the year period. Conclusion: It is essential to further develop the available intervention programs and increase their physical activity behavior. Planning such physical activity interventions for female population should involve aspects such as time, environmental variables and aerobic steps.Keywords: adults, pedometer, physical activity, step-count
Procedia PDF Downloads 3615933 The Effect of Mood and Creativity on Product Creativity: Using LEGO as a Hands-On Activity
Authors: Kaewmart Pongakkasira
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This study examines whether construction of LEGO reflects affective states and creativity as the clue to develop effective learning resources for classrooms. For this purpose, participants are instructed to complete a hands-on activity by using LEGO. Prior to the experiment, participants’ affective states and creativity are measured by the Positive and Negative Affect Schedule (PANAS) and the Alternate Uses Task (AUT), respectively. Then, subjects are asked to freely combine LEGO as unusual as possible versus constraint LEGO combination and named the LEGO products. Creativity of the LEGO products is scored for originality and abstractness of titles. It is hypothesized that individuals’ mood and creativity may affect product creativity. If so, there might be correlation among the three parameters.Keywords: affective states, creativity, hands-on activity, LEGO
Procedia PDF Downloads 3735932 An in vitro Evaluation of the Anthelmintic Activities of the Decoction and the Hexane-Soluble Extract and Its Fractions of the Aerial Part of Ruellia tuberosa Linn
Authors: Jeanne Phyre Lagare, Kirstin Rhys Pueblos
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This study was conducted to evaluate the possible anthelmintic activities of the decoction and the nonpolar constituents of the aerial part of Ruellia tuberosa Linn. against Eudrilus eugeniae or African Night Crawler earthworms as test organism which are of anatomic and physiological resemblance to the intestinal roundworm parasites of human beings. The in vitro anthelmintic assay of each extract was done by determining the time of paralysis and death of the test organisms at three concentrations (3, 25, 50 mg/mL). The hexane-soluble extract (RTH) showed better results compared to the decoction (RTD) at all concentrations employed. All the fractions of RTH showed significantly higher anthelmintic activities (111.43, 48.19, and 62.3 minutes, respectively) compared to their mother extract (164.56 minutes) at 3-mg/mL concentration. Moreover, RTH5 showed a comparable activity with the positive control mebendazole at 3-mg/mL concentration. Remarkably, fraction RTH4 exhibited the best anthelmintic activity at 3-mg/mL concentration for it showed the strongest anthelmintic activity than the rest of the test solutions tested. The study demonstrated the promising anthelmintic activity of the nonpolar constituent of the ethanolic extract of R. tuberosa Linn.Keywords: anthelmintic activity, Eudrillus eugenia, mebendazole, Ruellia tuberosa Linn
Procedia PDF Downloads 2015931 Study of the Antimicrobial Activity of the Extract of the Eucalyptus camaldulensis stemming from the Algerian Northeast
Authors: Meksem Nabila, Bordjiba Ouahiba, Meraghni Messaouda, Meksem Amara Leila, Djebar Mohhamed Reda
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The problems of protection of the cultures are being more and more important that they interest great number of farmers and scientists because of the excessive use of the organic phytosanitary products of synthesis that causes fatal damages on the environment. To reduce the inconveniences produced by these pesticides, the use of "biopesticides" originated from plants could be an alternative. The aim of this work is the valuation of a botanical species: Eucalyptus camaldulensis from Northeastern Algeria which extracts are supposed to have an antimicrobial activity, similar to pesticides. The extraction of secondary metabolites from the leaves of E. camaldulensis was realized using methanol and water, and measurements of total polyphenols were made by spectrometric method. Determination of the antimicrobial activity of the extracts at issue was realized in vitro on phyto-pathogenic fungal and bacterial stumps. Tests of comparison were included in the essays by using the chemical pesticidal products of synthesis. The obtained results show that the plant contains polyphenols with an efficiency mattering of the order of 22 %. These polyphenols have a strong fungicidal and bactericidal pesticidal activity against various microbial stumps and the values of the zones of inhibition are more important compared with that obtained in the presence of the chemicals of synthesis (fungicide).Keywords: eucalyptus camaldulensis, biopesticide, polyphenols, antimicrobial activity
Procedia PDF Downloads 4325930 Sterols Regulate the Activity of Phospholipid Scramblase by Interacting through Putative Cholesterol Binding Motif
Authors: Muhasin Koyiloth, Sathyanarayana N. Gummadi
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Biological membranes are ordered association of lipids, proteins, and carbohydrates. Lipids except sterols possess asymmetric distribution across the bilayer. Eukaryotic membranes possess a group of lipid translocators called scramblases that disrupt phospholipid asymmetry. Their action is implicated in cell activation during wound healing and phagocytic clearance of apoptotic cells. Cholesterol is one of the major membrane lipids distributed evenly on both the leaflet and can directly influence the membrane fluidity through the ordering effect. The fluidity has an impact on the activity of several membrane proteins. The palmitoylated phospholipid scramblases localized to the lipid raft which is characterized by a higher number of sterols. Here we propose that cholesterol can interact with scramblases through putative CRAC motif and can modulate their activity. To prove this, we reconstituted phospholipid scramblase 1 of C. elegans (SCRM-1) in proteoliposomes containing different amounts of cholesterol (Liquid ordered/Lo). We noted that the presence of cholesterol reduced the scramblase activity of wild-type SCRM-1. The interaction between SCRM-1 and cholesterol was confirmed by fluorescence spectroscopy using NBD-Chol. Also, we observed loss of such interaction when one of I273 in the CRAC motif mutated to Asp. Interestingly, the point mutant has partially retained scramblase activity in Lo vesicles. The current study elucidated the important interaction between cholesterol and SCRM-1 to fine-tune its activity in artificial membranes.Keywords: artificial membranes, CRAC motif, plasma membrane, PL scramblase
Procedia PDF Downloads 1755929 Anti-Inflammatory Activity of Lavandula antineae Maire from Algeria
Authors: Soumeya Krimat, Tahar Dob, Aicha Kesouri, Ahmed Nouasri, Hafidha Metidji
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Lavandula antineae Maire is an endemic medicinal plant of Algeria which is traditionally used for the treatment of chills, bruises, oedema and rheumatism. The objective of this study is to evaluate the anti-inflammatory of hydromethanolic aerial parts extract of Lavandula antineae for the first time using carrageenan-paw edema and croton oil-ear odema models. The plant extract, at the dose of 200 mg/kg, showed a significant anti-inflammatory activity (P˂0.05) in the carrageenan induced edema test in mice, showing 80.74% reduction in the paw thikness comparable to that produced by the standard drug aspirin 83.44% at 4h. When it was applied topically at a dosage of 1 and 2 mg per ear, the percent edema reduction in treated mice was 29.45% and 74.76%, respectively. These results demonstrate that Lavandula antineae Maire extract possess remarkable anti-inflammatory activity, supporting the folkloric usage of the plant to treat various inflammatory and pain diseases.Keywords: lavandula antineae maire, medicinal plant, anti-inflammatory activity, carrageenan-paw edema, croton oil-ear edema
Procedia PDF Downloads 3915928 Synthesis, Characterization and Antibacterial Activity of Metalloporphyrins: Role of Central Metal Ion
Authors: Belete B. Beyene, Ayenew M. Mihirteu, Misganaw T. Ayana, Amogne W. Yibeltal
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Modification of synthetic porphyrins is one of the promising strategies in an attempt to get molecules with desired properties and applications. Here in, we report synthesis, photophysical characterization and antibacterial activity of 5, 10, 15, 20-tetrakis-(4- methoxy carbonyl phenyl) porphyrin M(II); where M = Co, Fe, Ni, Zn. Metallation of the ligand was confirmed by using UV–Vis spectroscopy and ESI-Ms measurement, in which the number of Q bands in absorption spectra of the ligand decreased from four to one or two as a result of metal insertion to the porphyrin core. The antibacterial activity study of the complexes toward two Gram-positive (Staphylococcus aureus (S. aureus) and Streptococcus pyogenes (s. pyogenes)) and two Gram-negative (Escherichia coli (E. coli) and Klebsiella pneumoniae (K. pneumoniae)) bacteria by disc diffusion method showed a promising inhibitory activity. The complexes exhibited highest activities at highest concentration and were better than the activity of free base ligand, the salts, and blank solution. This could be explained on the basis of Overton's concept of cell permeability and Tweed's Chelation theory. An increased lipo-solubility enhances the penetration of the complexes into the lipid membrane and interferes with the normal activities of the bacteria. Our study, therefore, showed that the growth inhibitory effect of these metalloporphyrins is generally in order of ZnTPPCOOMe > NiTPPCOOMe > CoTPPCOOMe> FeTPPCOOMe, which may be attributed to the better lipophilicity and binding of the complex with the cellular components.Keywords: porphyrins, metalloporphyrins, spectral property, antibacterial activity, synthesis
Procedia PDF Downloads 735927 Evaluation of Central Nervous System Activity of Synthesized 5, 5-Diphenylimidazolidine-2, 4-Dione Derivatives
Authors: Shweta Verma
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Background: Epilepsy is a chronic non-communicable central nervous system (CNS) disorder which affects a large population of all ages. Different classes of drugs are used for the treatment of this neurological disorder, but due to augmented drug resistance and side effects, these drugs become incompetent. Therefore, we design the synthesis of ten new derivatives of Phenytoin. The moiety of Phenytoin was hybridized with different phenols by using three step approach. The synthesized molecules were then investigated for different physicochemical parameters, such as Log P values using diverse software programs and to predict the potential to cross the blood-brain barrier. Objective: The Phenytoin derivatives were designed, synthesized, and characterized to meet the structural necessities indispensable for antiepileptic activity. Method: Firstly, the chloroacetylation of the 5,5-diphenyl hydantoin was carried out, and then various substituted phenols were added to it. The synthesized compounds were characterized and evaluated for antianxiety activity by elevated plus maze method and antiepileptic activity by using subcutaneous pentylenetetrazole (scPTZ) and maximal electroshock (MES) models and neurotoxicity. Result: The number of derivatives of 5,5-diphenyl hydantoin was developed and optimized. The number of parameters was optimized which reveal that the compound containing chloro group such as C3 and C6 showed imperative potential when compared with the standard drug Diazepam. Other compounds containing nitro and methyl group were also found to possess activity. Conclusion: It was summarized that the new compounds of 5,5-diphenyl hydantoin derivatives were synthesized. The results of the data show that the compound containing chloro group is more potent for CNS activity. The new compounds have the probability of being optimized further to engender new scaffolds to treat various CNS disorders.Keywords: phenytoin, parameters, CNS activity, blood-brain barrier, Log P, CNS active
Procedia PDF Downloads 725926 Anticancer Lantadene Derivatives: Synthesis, Cytotoxic and Docking Studies
Authors: A. Monika, Manu Sharma, Hong Boo Lee, Richa Dhingra, Neelima Dhingra
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Nuclear factor-κappa B serve as a molecular lynchpin that links persistent infections and chronic inflammation to increased cancer risk. Inflammation has been recognized as a hallmark and cause of cancer. Natural products present a privileged source of inspiration for chemical probe and drug design. Herbal remedies were the first medicines used by humans due to the many pharmacologically active secondary metabolites produced by plants. Some of the metabolites like Lantadene (pentacyclic triterpenoids) from the weed Lantana camara has been known to inhibit cell division and showed anti-antitumor potential. The C-3 aromatic esters of lantadenes were synthesized, characterized and evaluated for cytotoxicity and inhibitory potential against Tumor necrosis factor alpha-induced activation of Nuclear factor-κappa B in lung cancer cell line A549. The 3-methoxybenzoyloxy substituted lead analogue inhibited kinase activity of the inhibitor of nuclear factor-kappa B kinase in a single-digit micromolar concentration. At the same time, the lead compound showed promising cytotoxicity against A549 lung cancer cells with IC50 ( half maximal inhibitory concentration) of 0.98l µM. Further, molecular docking of 3-methoxybenzoyloxy substituted analogue against Inhibitor of nuclear factor-kappa B kinase (Protein data bank ID: 3QA8) showed hydrogen bonding interaction involving oxygen atom of 3-methoxybenzoyloxy with the Arginine-31 and Glutamine-110. Encouraging results indicate the Lantadene’s potential to be developed as anticancer agents.Keywords: anticancer, lantadenes, pentacyclic triterpenoids, weed
Procedia PDF Downloads 1565925 Cytotoxic, Antimicrobial and Antiviral Activities of Acovenoside A: A Cardenolide Isolated from an Egyptian Cultivar of Acokanthera spectabilis Leaves
Authors: Howaida I. Abd-Alla, Amal Z. Hassan, Maha Soltan, Atef G. Hanna, Mounir M. El-Safty
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Acokanthera oblongifolia (Apocynaceae) is used for treatment of several infection diseases and is a well-known cardiac glycoside-containing plant. The infusion of their leaves is gargled to treat tonsillitis and is used medicinally to treat snakebites. The total cardiac glycosides content in the leaves was determined by referring to gitoxigenin as a reference compound. Two triterpenes, lup-20(29)-en-3β-ol (1) and oleanolic acid (2); two cardenolides, acovenoside A (3) and acobioside A (4) were isolated from the ethyl acetate extract. Their structures were determined on the basis of spectral analysis. Major constituents isolated from this species were evaluated for cytotoxicity against normal lung cell line (Wi38) and antimicrobial activities against Gram-positive (two strains) and Gram-negative bacteria (four strains), yeast-like fungi (two strains) and fungi (five strains). The minimum inhibitory concentration (MIC) of the compounds was determined using broth microdilution method. Their viral inhibitory effects against avian influenza virus type A (AI-H5N1) and Newcastle disease virus (NDV) in specific pathogen free (SPF) embryonated chicken eggs (ECE), chicken embryo fibroblasts (CEF) and Vero cells were evaluated. The cardenolide (3) showed viral inhibitory effects against AI-H5N1 and NDV in SPF ECE. The two cardenolides isolated have shown potent cytotoxicity against Vero cells. Compound (3) showed potent anti-Gram-negative bacteria activity. These results suggested that acovenoside A might be promising for future antiviral and antimicrobial drug design.Keywords: Acokanthera, AI-H5N1, Cardenolides, NDV, SPF-ECE, VERO, Wi38 , Microbe
Procedia PDF Downloads 1785924 Assessment of Physical Activity Levels in Qatar: A Pedometer-Based Study
Authors: Souzan Al Sayegh, Izzeldin Ibrahim, Mercia Van Der Walt, Mohamed Al-Kuwari
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Background: Walking is the most common form of physical activity which can promote a healthy well-being among people of different age groups. In this regard, pedometers are becoming more popular within research and are considered useful tools in monitoring physical activity levels based on individuals’ daily steps. A value of ˂5,000 steps/day is identified as a sedentary lifestyle index where individuals are physically inactive. Those achieving 5,000-7,499 steps/day have a low active lifestyle as they do not meet the moderate-to-vigorous physical activity (MVPA) recommendations. Moreover, individuals achieving ≥7,500 steps/day are classified as physically active. The objective of this study is to assess the physical activity levels of adult population in Qatar through a pedometer-based program over a one-year period. Methods: A cross-sectional analysis, as part of a longitudinal study, was carried out over one year to assess the daily step count. 'Step into Health' is a community-based program launched by Aspire as an approach for the purpose of improving physical activity across the population of Qatar. The program involves the distribution of pedometers to registered members which is supported by a self-monitoring online account and linked to a web database. Daily habitual physical activity (daily total step count) was assessed through Omron HJ-324U pedometer. Analyses were done on data extracted from the web database. Results: A total of 1,988 members were included in this study (males: n=1,143, 57%; females: n=845, 43%). Average age was 37.8±10.9 years distributed as 60% of age between age 25-54 (n=1,186), 27% of age 45-64 (n=546), and 13% of age 18-24 years (n=256). Majority were non-Qataris, 81% (n=1,609) compared with 19% of the Qatari nationality (n=379). Average body mass index (BMI) was 27.8±6.1 (kg/m2) where most of them (41%, n=809) were found to be overweight, between 25-30 kg/m2. Total average step count was 5,469±3,884. Majority were found to be sedentary (n=1110, 55.8%). Middle aged individuals were more active than the other two age groups. Males were seen as more active than females. Those who were less active had a higher BMI. Older individuals were more active. There was a variation in the physical activity level throughout the year period. Conclusion: It is essential to further develop the available intervention programs and increase their physical activity behavior. Planning such physical activity interventions for female population should involve aspects such as time, environmental variables and aerobic steps.Keywords: adults, pedometer, physical activity, step-count
Procedia PDF Downloads 3065923 Leisure Time Physical Activity Patterns in Odisha, India
Authors: Shankar Ganesh, Rishee Patel, Vikram Dwivedi, Balakishore P., Deepak Chhabra, Anandhi Dakshinamoorthy, Parminder Kaur
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Background: The World Health Organization has recommended a moderate intensity physical activity of 150 minutes, or 75 minutes vigorous-intensity physical activity per week to achieve optimal health benefits. It is not known if Indian public who indulge in leisure time physical exercises satisfy these recommendations. Methods: This study used a questionnaire to obtain data regarding demographic details, current engagement in leisure time physical activities, and dosages of these exercises from participants between 18-64 years of age. Results: Data was collected from a total of 390 participants (231 males and 159 females). 50.76% and 34.35% o of the participants reported exercising voluntarily and for health benefits respectively. Most participants (94.61%) indicated exercising without prescription. 55.38% and 12.82% of the participants under and above 38 years of age perform moderate to vigorous intensity exercises respectively. Conclusion: The over-all results of this study indicate that the participants’ choices of leisure time physical exercises are based on their personal choices and beliefs. The exercise intensities undertaken do not meet the global recommended intensities, especially in those above 38 years of age. Professionals and facilities to engage the public in the WHO recommended intensities of physical activity needs to be established.Keywords: physical activity, exercise, India, sedentary
Procedia PDF Downloads 2405922 The Effectiveness of Incidental Physical Activity Interventions Compared to Other Interventions in the Management of People with Low Back Pain: A Systematic Review and Meta-Analysis
Authors: Hosam Alzahrani, Martin Mackey, Emmanuel Stamatakis, Marina B. Pinheiro, Manuela Wicks, Debra Shirley
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Objective: To investigate the effectiveness of incidental (non-structured) physical activity interventions compared with other commonly prescribed interventions for the management of people with low back pain (LBP). Methods: We performed a systematic review with meta-analyses of eligible randomized controlled trials obtained by searching Medline, Scopus, CINAHL, EMBASE, and CENTRAL. This review considered trials investigating the effect of incidental physical activity interventions compared to other interventions in people aged 18 years or over, diagnosed with non-specific LBP. Analyses were conducted separately for short-term (≤3 months), intermediate-term (> 3 and < 12 months), and long-term (≥ 12 months), for each outcome. The analyses were conducted using the weighted mean difference (WMD). The overall quality of evidence was assessed using the GRADE system. Meta-analyses were only performed for pain and disability outcomes as there was insufficient data on the other outcomes. Results: For pain, the pooled results did not show any significant effects between the incidental physical activity intervention and other interventions at any time point. For disability, incidental physical activity was not statistically more effective than other interventions at short-term; however, the pooled results favored incidental physical activity at intermediate-term (WMD= -6.05, 95% CI: -10.39 to -1.71, p=0.006) and long-term (WMD= -6.40 95% CI: -11.68 to -1.12, p=0.02) follow-ups among participants with chronic LBP. The overall quality of evidence was rated “moderate quality” based on the GRADE system. Conclusion: The incidental physical activity intervention provided intermediate and long disability relief for people with chronic LBP, although this improvement was small and not likely to be clinically important.Keywords: physical activity, incidental, low back pain, systematic review, meta-analysis
Procedia PDF Downloads 1575921 Isolation, Structure Elucidation, and Biological Evaluation of Acetylated Flavonoid Glycosides from Centaurium spicatum
Authors: Abdelaaty A. Shahat, Mansour S. Alsaid
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Four Acetylated flavonol glycosides were isolated from Centaurium spicatum (L.) Fritsch (Gentianaceae). Structure elucidation, especially the localization of the acetyl groups, and complete 1H and 13C NMR assignments of these biologically active compounds were carried out using one- and two-dimensional NMR methods, including CNMR, DEPT-135 and DEPT-90 and gradient-assisted experiments such as DQF-COSY, TOCSY, HSQC and HMBC experiments. The antioxidant activities of the new acetylated flavonoid glycosides using DPPH• assay were determined. The compounds tested showed a good DPPH• activity compared with control, but their activity was lower than that of their corresponding aglycone, quercetin.Keywords: Centaurium spicatum, flavonoids, biological activity, isolation, glycosides
Procedia PDF Downloads 4075920 Assessment of Hemostatic Activity of the Aqueous Extract of Leaves of Marrubium vulgare L.: A Mediterranean Lamiaceae Algeria
Authors: Nabil Ghedadba, Abdessemed Samira, Leila Hambaba, Sidi Mohamed Ould Mokhtar, Nassima Fercha, Houas Bousselsela
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The overall objective of this study was to evaluate in vitro the hemostatic activity of secondary metabolites (polyphenols, flavonoids, and tannins) of Marrubium vulgare leaves, aromatic plant widely used in traditional medicine for the treatment of asthma, cough, diabetes (by its effect on the pancreas to secrete insulin), heart disease, fever has a high efficiency as against inflammation. Qualitative analysis of the aqueous extract (AQE) by thin layer chromatography revealed the presence of quercetin, kaempferol and rutin. Quantification of total phenols by Folin Ciocalteu method and flavonoids by AlCl3 method gave high values with AQE: 175±0.80 mg GAE per 100g of the dry matter, 23.86±0.36 mg QE per 100g of dry matter. Moreover, the assay of condensed tannins by the vanillin method showed that AQE contains the highest value: 16.55±0.03 mg e-catechin per 100 g of dry matter. Assessment of hemostatic activity by the plasma recalcification method (time of Howell) has allowed us to discover the surprising dose dependent anticoagulant effect of AQE lyophilized from leaves of M. vulgare. A positive linear correlation between the two parameters studied: the content of condensed tannins and hemostatic activity (r=0.96) were used to highlight a possible role of these compounds that are potent vasoconstrictor activity in hemostatic. From these results we can see that Marrubium vulgre could be used for the treatment of health.Keywords: Marrubium vulgare L., aqueous extract, phenolic compounds dosing, hemostatic activity, condensed tannins
Procedia PDF Downloads 2425919 Antitrypanosomal Activity of Stigmasterol: An in silico Approach
Authors: Mohammed Auwal Ibrahim, Aminu Mohammed
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Stigmasterol has previously been reported to possess antitrypanosomal activity using in vitro and in vivo models. However, the mechanism of antitrypanosomal activity is yet to be elucidated. In the present study, molecular docking was used to decipher the mode of interaction and binding affinity of stigmasterol to three known antitrypanosomal drug targets viz; adenosine kinase, ornithine decarboxylase and triose phosphate isomerase. Stigmasterol was found to bind to the selected trypanosomal enzymes with minimum binding energy of -4.2, -6.5 and -6.6 kcal/mol for adenosine kinase, ornithine decarboxylase, and triose phosphate isomerase respectively. However, hydrogen bond was not involved in the interaction of stigmasterol with all the three enzymes, but hydrophobic interaction seemed to play a vital role in the binding phenomenon which was predicted to be non-competitive like type of inhibition. It was concluded that binding to the three selected enzymes, especially triose phosphate isomerase, might be involved in the antitrypanosomal activity of stigmasterol but not mediated via a hydrogen bond interaction.Keywords: antitrypanosomal, in silico, molecular docking, stigmasterol
Procedia PDF Downloads 2785918 Factors Associated with Involvement in Physical Activity among Children (Aged 6-18 Years) Training at Excel Soccer Academy in Uganda
Authors: Syrus Zimaze, George Nsimbe, Valley Mugwanya, Matiya Lule, Edgar Watson, Patrick Gwayambadde
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Physical inactivity is a growing global epidemic, also recognised as a major public health challenge. Globally, there are alarming rates of children reported with cardiovascular disease and obesity with limited interventions. In Sub Saharan Africa, there is limited information about involvement in physical activity especially among children aged 6 to 18 years. The aim of this study was to explore factors associated with involvement in physical activity among children in Uganda. Methods: We included all parents with children aged 6 to 18 years training with Excel Soccer Academy between January 2017 and June 2018. Physical activity definition was time spent participating in routine soccer training at the academy for more than 30 days. Each child's attendance was recorded, and parents provided demographic and social economic data. Data on predictors of physical activity involvement were collected using a standardized questionnaire. Descriptive statistics and frequency were used. Binary logistic regression was used at the multi variable level adjusting for education, residence, transport means and access to information technology. Results: Overall 356 parents were interviewed; Boys 318 (89.3%) engaged more in physical activity than girls. The median age for children was 13 years (IQR:6-18) and 42 years (IQR:37-49) among parents. The median time spent at the Excel soccer academy was 13.4 months (IQR: 4.6-35.7) Majority of the children attended formal education, p < 0.001). Factors associated with involvement in physical activity included: owning a permanent house compared to a rented house (odds ratio [OR] :2.84: 95% CI: 2.09-3.86, p < 0.0001), owning a car compared to using public transport (OR: 5.64 CI: 4.80-6.63, p < 0.0001), a parent having received formal education compared to non-formal education (OR: 2.93 CI: 2.47-3.46, p < 0.0001) and daily access to information technology (OR:0.40 CI:0.25-0.66, p < 0.001). Parent’s age and gender were not associated to involvement in physical activity. Conclusions: Socioeconomic factors were positively associated with involvement in physical activity with boys participating more than girls in soccer activities. More interventions are required geared towards increasing girl’s participation in physical activity and those targeting children from less privilege homes.Keywords: physical activity, Sub-Saharan Africa, social economic factors, children
Procedia PDF Downloads 1665917 Lightweight Hybrid Convolutional and Recurrent Neural Networks for Wearable Sensor Based Human Activity Recognition
Authors: Sonia Perez-Gamboa, Qingquan Sun, Yan Zhang
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Non-intrusive sensor-based human activity recognition (HAR) is utilized in a spectrum of applications, including fitness tracking devices, gaming, health care monitoring, and smartphone applications. Deep learning models such as convolutional neural networks (CNNs) and long short term memory (LSTM) recurrent neural networks (RNNs) provide a way to achieve HAR accurately and effectively. In this paper, we design a multi-layer hybrid architecture with CNN and LSTM and explore a variety of multi-layer combinations. Based on the exploration, we present a lightweight, hybrid, and multi-layer model, which can improve the recognition performance by integrating local features and scale-invariant with dependencies of activities. The experimental results demonstrate the efficacy of the proposed model, which can achieve a 94.7% activity recognition rate on a benchmark human activity dataset. This model outperforms traditional machine learning and other deep learning methods. Additionally, our implementation achieves a balance between recognition rate and training time consumption.Keywords: deep learning, LSTM, CNN, human activity recognition, inertial sensor
Procedia PDF Downloads 1505916 Work, Pension and Physical Activity: Findings from an Interview Study
Authors: Sonia Lippke, Eric Rost, Volker Cihlar
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Objective: To examine the interrelation of physical activity with work-related variables in older individuals to determine pathways to promote the maintenance of an aging workforce’s ability and motivation to work. Design/methodology/approach: An interview-study was conducted with N=5,002 community-dwelling people aged 55 to 70 years (for T1). N=2,501 (50%) were interviewed 3 years later again (T2). Correlation-, Chi²-, MANOVA and moderated mediation analyses were performed. Findings: The less people worked, the more physically active they were. Working was only related to calendar age but not to subjective age. Men and women only differed in working hours and an interaction of gender and pension regarding working hours and subjective health revealed: Controlled for calendar age, the amount of worked hours while receiving pension was about the same in men and women, however, men worked significantly more hours if they did not receive pension. The relationship between physical activity and worked hours was mediated by life investment and subjective health in women, and by subjective health in men. Practical implications: Developing good health through performing physical activity should be done as part of work-place health promotion or by work organization and HR management to enable, and motivate older individuals to work even when receiving pension. Thus, such initiates should not only offered for younger and middle aged employees. Physical activity and company-facilitated sports activities can be an integral part in this. Originality/value: This is the first study testing these mechanisms in this age group, indicating the importance of not only understanding physical activity as a time challenge to work but also the potential to protect workability and to work aside from receiving pension.Keywords: life investment, moderated mediation, physical activity, older workers, subjective health
Procedia PDF Downloads 3025915 Assessment of Physical Activity Patterns in Patients with Cardiopulmonary Diseases
Authors: Ledi Neçaj
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Objectives: The target of this paper is (1) to explain objectively physical activity model throughout three chronic cardiopulmonary conditions, and (2) to study the connection among physical activity dimensions with disease severity, self-reported physical and emotional functioning, and exercise performance. Material and Methods: This is a cross-sectional study of patients in their domestic environment. Patients with cardiopulmonary diseases were: chronic obstructive pulmonary disease (COPD), (n-63), coronary heart failure (n=60), and patients with implantable cardioverter defibrillator (n=60). Main results measures: Seven ambulatory physical activity dimensions (total steps, percentage time active, percentage time ambulating at low, medium, and hard intensity, maximum cadence for 30 non-stop minutes, and peak performance) have been measured with an accelerometer. Results: Subjects with COPD had the lowest amount of ambulatory physical activity compared with topics with coronary heart failure and cardiac dysrhythmias (all 7 interest dimensions, P<.05); total step counts have been: 5319 as opposed to 7464 as opposed to 9570, respectively. Six-minute walk distance becomes correlated (r=.44-.65, P<.01) with all physical activity dimensions inside the COPD pattern, the most powerful correlations being with total steps and peak performance. In topics with cardiac impairment, maximal oxygen intake had the most effective small to slight correlations with five of the physical activity dimensions (r=.22-.40, P<.05). In contrast, correlations among 6-minute walk test distance and physical activity have been higher (r=.48-.61, P<.01) albeit in a smaller pattern of most effective patients with coronary heart failure. For all three samples, self-reported physical and mental health functioning, age, frame mass index, airflow obstruction, and ejection fraction had both exceptionally small and no significant correlations with physical activity. Conclusions: Findings from this study present a profitable benchmark of physical activity patterns in individuals with cardiopulmonary diseases for comparison with future studies. All seven dimensions of ambulatory physical activity have disfavor between subjects with COPD, heart failure, and cardiac dysrhythmias. Depending on the research or clinical goal, the use of one dimension, such as total steps, may be sufficient. Although physical activity had high correlations with performance on a six-minute walk test relative to other variables, accelerometers-based physical activity monitoring provides unique, important information about real-world behavior in patients with cardiopulmonary not already captured with existing measures.Keywords: ambulatory physical activity, walking, monitoring, COPD, heart failure, implantable defibrillator, exercise performance
Procedia PDF Downloads 875914 Analyzing Doctors’ Knowledge of the United Kingdom Chief Medical Officer's Guidelines for Physical Activity: Survey of Secondary Care Doctors in a District General Hospital
Authors: Alexandra Von Guionneau, William Sloper, Charlotte Burford
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The benefits of exercise for the prevention and management of chronic disease are well established and the importance of primary care practitioners in promoting exercise is becoming increasingly recognized. However, those with severe manifestations of the chronic disease are managed in a secondary care setting. Secondary care practitioners, therefore, have a role to play in promoting physical activity. Methods: In order to assess secondary care doctors’ knowledge of the Chief Medical Officer’s guidelines for physical activity, a 12-question survey was administered to staff working in a district general hospital in South England during team and unit meetings. Questions related to knowledge of the current guidelines for both 19 - 64 year olds and older adults (65 years and above), barriers to exercise discussion or prescription and doctors’ own exercise habits. Responses were collected anonymously and analyzed using SPSS Version 24.0. Results: 96 responses were collected. Doctors taking part in the survey ranged from foundation years (26%) to consultants (40%). 17.7% of participants knew the guidelines for moderate intensity activity for 19 - 64 year olds. Only one participant knew all of the guidance for both 19 - 64 year olds and older adults. While 71.6% of doctors felt they were adequately informed about how to exercise, only 45.6% met the minimum recommended guidance for moderate intensity activity. Conclusion: More work is needed to promote the physical activity guidelines and exercise prescription to doctors working within a secondary care setting. In addition, doctors require more support to personally meet the recommended minimum level of physical activity.Keywords: exercise is medicine, exercise prescription, physical activity guidelines, exercise habits
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