Search results for: antitumor activity
6081 Evaluation of Moroccan Microalgae Spirulina platensis as a Potential Source of Natural Antioxidants
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
Procedia PDF Downloads 1656080 LIFirr with an Indicator of Microbial Activity in Paraffinic Oil
Authors: M. P. Casiraghi, C. M. Quintella, P. Almeida
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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
Procedia PDF Downloads 5236079 Walnut (Juglans Regia) Extracts: Investigation of Antioxidant Effect, Total Phenols and Tyrosinase Inhibitory Activity
Authors: N. Saki, S. Nalbantoglu, M. Akin, G. Arabaci
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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
Procedia PDF Downloads 3016078 Synthesis and Antiproliferative Activity of 5-Phenyl-N3-(4-fluorophenyl)-4H-1,2,4-triazole-3,4-diamine Derivatives
Authors: L. Mallesha, P. Mallu, B. Veeresh
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In the present study, 2, 6-diflurobenzohydrazide and 4-fluorophenylisothiocyanate were used as the starting materials to synthesize 5-phenyl-N3-(4-fluorophenyl)-4H-1, 2, 4-triazole-3, 4-diamine. Further, compound 5-phenyl-N3-(4-fluorophenyl)-4H-1, 2, 4-triazole-3,4-diamine reacted with fluoro substituted benzaldehydes to yield a series of Schiff bases. All the final compounds were characterized using IR, 1H NMR, 13C NMR, MS and elemental analyses. New compounds were evaluated for their antiproliferative effect using the MTT assay method against four human cancer cell lines (K562, COLO-205, MDA-MB231, and IMR-32) for the time period of 24 h. Among the series, few compounds showed good activity on all cell lines, whereas the other compounds in the series exhibited moderate activity.Keywords: Schiff bases, MTT assay, antiproliferative activity, human cancer cell lines, 1, 2, 4-triazoles
Procedia PDF Downloads 3726077 Microwave-Assisted Synthesis of a Class of Pyridine and Purine Thioglycoside Analogs
Authors: Mamdouh Abu-Zaied, K. Mohamed, Galal A. Nawwar
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Microwave-assisted synthesis of a new class of pyridine or purine thioglycoside analogs from readily available starting materials has been described. The key step of this protocol is the formation of sodium pyridine 4-thiolate 4 and pyrazolo[1,5-a]pyrimidine-7-thiolate 5 derivatives via condensation of 1 with cyanoacetanilide derivative 2 or 5-aminopyrazole derivative 3 respectively under microwave irradiation, followed by coupling with halo sugars to give the corresponding pyridine and purine thioglycoside analogs. The obtained compounds were evaluated in vitro against lung (A549), colon (HCT116), liver (HEPG2), and MCF-7(breast) cancer cell lines. Some of them recorded promising activities.Keywords: antitumor, cyclic sugars, pyrazoles, pyridines, pyrimidines, purines, thioglycosides
Procedia PDF Downloads 2406076 Phytochemical Study and Biological Activity of Sage (Salvia officinalis L.)
Authors: Mekhaldi Abdelkader, Bouzned Ahcen, Djibaoui Rachid, Hamoum Hakim
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This study presents an attempt to evaluate the antioxidant and antimicrobial activity of methanolic extract and essential oils prepared from the leaves of sage (Salvia officinalis L.). The content of polyphenols in the methanolic extract of the leaves from Salvia officinalis extract was determined by spectrophoto- metrically, calculated as gallic acid and catechin equivalent. Antioxidant activity was evaluated by free radical scavenging activity using 2,2-diphenylpicryl-1-picrylhydrazyl (DPPH) assay. The plant essential oil and methanol extract were also subjected to screenings for the evaluation of their antioxidant activities using 2, 2-diphenyl-1-picrylhydrazyl (DPPH) test. While the plant essential oil showed only weak antioxidant activities, its methanol extract was considerably active in DPPH (IC50= 37.29µg/ml) test. Appreciable total phenolic content (31.25mg/g) was also detected for the plant methanol extract as gallic acid equivalent in the Folin–Ciocalteu test. The plant was also screened for its antimicrobial activity and good to moderate inhibitions were recorded for its essential oil and methanol extract against most of the tested microorganisms. The present investigation revealed that this plant has rich source of antioxidant properties. It is for this reason that sage has found increasing application in food formulations.Keywords: antibacterial activity, antioxidant activity, flavonoid, polyphenol, salvia officinalis
Procedia PDF Downloads 4086075 Rationally Designed Dual PARP-HDAC Inhibitor Elicits Striking Anti-leukemic Effects
Authors: Amandeep Thakur, Yi-Hsuan Chu, Chun-Hsu Pan, Kunal Nepali
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The transfer of ADP-ribose residues onto target substrates from nicotinamide adenine dinucleotide (NAD) (PARylation) is catalyzed by Poly (ADP-ribose) polymerases (PARPs). Amongst the PARP family members, the DNA damage response in cancer is majorly regulated by PARP1 and PARP2. The blockade of DNA repair by PARP inhibitors leads to the progression of DNA single-strand breaks (induced by some triggering factors) to double-strand breaks. Notably, PARP inhibitors are remarkably effective in cancers with defective homologous recombination repair (HRR). In particular, cancer cells with BRCA mutations are responsive to therapy with PARP inhibitors. The aforementioned requirement for PARP inhibitors to be effective confers a narrow activity spectrum to PARP inhibitors, which hinders their clinical applicability. Thus, the quest to expand the application horizons of PARP inhibitors beyond BRCA mutations is the need of the hour. Literature precedents reveal that HDAC inhibition induces BRCAness in cancer cells and can broaden the therapeutic scope of PARP inhibitors. Driven by such disclosures, dual inhibitors targeting both PARP and HDAC enzymes were designed by our research group to extend the efficacy of PARP inhibitors beyond BRCA-mutated cancers to cancers with induced BRCAness. The design strategy involved the installation of Veliparib, an investigational PARP inhibitor, as a surface recognition part in the HDAC inhibitor pharmacophore model. The chemical architecture of veliparib was deemed appropriate as a starting point for the generation of dual inhibitors by virtue of its size and structural flexibility. A validatory docking study was conducted at the outset to predict the binding mode of the designed dual modulatory chemical architectures. Subsequently, the designed chemical architectures were synthesized via a multistep synthetic route and evaluated for antitumor efficacy. Delightfully, one compound manifested impressive anti-leukemic effects (HL-60 cell lines) mediated via dual inhibition of PARP and class I HDACs. The outcome of the western blot analysis revealed that the compound could downregulate the expression levels of PARP1 and PARP2 and the HDAC isoforms (HDAC1, 2, and 3). Also, the dual PARP-HDAC inhibitor upregulated the protein expression of the acetyl histone H3, confirming its abrogation potential for class I HDACs. In addition, the dual modulator could arrest the cell cycle at the G0/G1 phase and induce autophagy. Further, polymer-based nanoformulation of the dual inhibitor was furnished to afford targeted delivery of the dual inhibitor at the cancer site. Transmission electron microscopy (TEM) results indicate that the nanoparticles were monodispersed and spherical. Moreover, the polymeric nanoformulation exhibited an appropriate particle size. Delightfully, pH-sensitive behavior was manifested by the polymeric nanoformulation that led to selective antitumor effects towards the HL-60 cell lines. In light of the magnificent anti-leukemic profile of the identified dual PARP-HDAC inhibitor, in-vivo studies (pharmacokinetics and pharmacodynamics) are currently being conducted. Notably, the optimistic findings of the aforementioned study have spurred our research group to initiate several medicinal chemistry campaigns to create bifunctional small molecule inhibitors addressing PARP as the primary target.Keywords: PARP inhibitors, HDAC inhibitors, BRCA mutations, leukemia
Procedia PDF Downloads 236074 Phytochemical Profiles and Antioxidant Activity of Selected Indigenous Vegetables in Northern Mindanao, Philippines
Authors: Renee P. Baang, Romeo M. del Rosario, Nenita D. Palmes
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The crude methanol extracts of five indigenous vegetables namely, Amarathus tricolor, Basella rubra L, Chochurus olitorius L., Ipomea batatas, and Momordica chuchinensis L., were examined for their phytochemical profile and antioxidant activity using 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical. The values for DPPH radical scavenging activity ranged from 7.6-89.53% with B. rubra and I. batatas having the lowest and highest values, respectively. The total flavonoid content of all five indigenous vegetables ranged from 74.65-277.3 mg quercetin equivalent per gram of dried vegetable material while the total phenolic content ranged from 1.93-6.15 mg gallic acid equivalent per gram dried material. Phytochemical screening revealed the presence of steroids, flavonoids, saponins, tannins, carbohydrates and reducing sugars, which may also be associated with the antioxidant activity shown by these indigenous vegetables.Keywords: antioxidant, DPPH radical scavenging activity, Philippine İndigenous vegetables, phytochemical screening
Procedia PDF Downloads 3336073 Validity of Clinical Disease Activity Index (CDAI) to Evaluate the Disease Activity of Rheumatoid Arthritis Patients in Sri Lanka: A Prospective Follow up Study Based on Newly Diagnosed Patients
Authors: Keerthie Dissanayake, Chandrika Jayasinghe, Priyani Wanigasekara, Jayampathy Dissanayake, Ajith Sominanda
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The routine use of Disease Activity Score-28 (DAS28) to assess the disease activity in rheumatoid arthritis (RA) is limited due to its dependency on laboratory investigations and the complex calculations involved. In contrast, the clinical disease activity index (CDAI) is simple to calculate, which makes the "treat to target" strategy for the management of RA more practical. We aimed to assess the validity of CDAI compared to DAS28 in RA patients in Sri Lanka. A total of 103 newly diagnosed RA patients were recruited, and their disease activity was calculated using DAS 28 and CDAI during the first visit to the clinic (0 months) and re-assessed at 4 and 9 months of the follow-up visits. The validity of the CDAI, compared to DAS 28, was evaluated. Patients had a female preponderance (6:1) and a short symptom duration (mean = 6.33 months). The construct validity of CDAI, as assessed by Cronbach's α test, was 0.868. Convergent validity was assessed by correlation and Kappa statistics. Strong positive correlations were observed between CDAI and DAS 28 at the baseline (0 months), 4, and 9 months of evaluation (Spearman's r = 0.9357, 0.9354, 0.9106, respectively). Moderate-good inter-rater agreements between the DAS-28 and CDAI were observed (Weighted kappa of 0.660, 0.519, and 0.741 at 0, 4, and 9 months respectively). Discriminant validity, as assessed by ROC curves at 0, 4th, and 9th months of the evaluation, showed the area under the curve (AUC) of 0.958, 0.985, and 0.914, respectively. The suggested cut-off points for different CDAI disease activity categories according to ROC curves were ≤ 2 (Remission), >2 to ≤ 5 (low), >5 to ≤ 18 (moderate), > 18 (high). These findings indicate that the CDAI has good concordance with DAS 28 in assessing the disease activity in RA patients in this study sample.Keywords: rheumatoid arthritis, CDAI, disease activity, Sri Lanka, validation
Procedia PDF Downloads 1546072 Anti-inflammatory and Antioxidant Activity of Heliotropium indicum Linn. Used for Cancer Patients Treatment
Authors: Jitpisute Chunthorng-Orn, Thana Juckmeta, Onmanee Prajuabjinda, Arunporn Itharat
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Inflammation and oxidative stress work together to produce symptoms in cancer patients. The whole part of it is used as a preparation to treat cancer patients in Khampramong temple which has been a place of treatment and palliative care for cancer patients since 2005. Thus, the objective of this study was to investigate anti-inflammatory and antioxidant activities of Heliotropium indicum extracts. Dried plant materials were extracted in a similar manner to those practiced by the Khampramong Temple i.e. maceration in 95% ethanol and boiling in water. For anti-inflammation activity, both extracts were tested for suppression of nitric oxide (NO) production in LPS-induced RAW 264.7 cells. They were also tested for antioxidant activity by DPPH radical scavenging assay. This study found that the ethanolic extract of Heliotropium indicum exhibited higher inhibitory activity of NO release than Indomethacin as a positive control (IC50 value of 24.17±2.12 and 34.67±6.23 μg/mL, respectively). For DPPH radical scavenging assay, the ethanolic extract also exhibited antioxidant activity but less than BHT as a antioxidant compound (EC50 values = 28.91±4.26 and 13.08±0.29 μg/mL, respectively). In contrast, its water extract had no inhibitory activity on NO release (IC50 > 100 μg/mL) and no inhibitory activity on DPPH radicals (EC50 values > 100 μg/mL). The results showed correlation between anti-inflammation and antioxidant activity and these results also support using this plant to treat cancer patients.Keywords: Heliotropium indicum, RAW 264.7, DPPH, Khampramong Temple
Procedia PDF Downloads 5386071 Synthesis, Characterization, and Biological Evaluation of 1,3,4-Mercaptooxadiazole Ether Derivatives Analogs as Antioxidant, Cytotoxic, and Molecular Docking Studies
Authors: Desta Gebretekle Shiferaw, Balakrishna Kalluraya
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Oxadiazoles and their derivatives with thioether functionalities represent a new and exciting class of physiologically active heterocyclic compounds. Several molecules with these moieties play a vital role in pharmaceuticals because of their diverse biological activities. This paper describes a new class of 1,3,4- oxadiazole-2-thioethers with acetophenone, coumarin, and N-phenyl acetamide residues (S-alkylation), with the hope that the addition of various biologically active molecules will have a synergistic effect on anticancer activity. The structure of the synthesized title compounds was determined by the combined methods of IR, proton-NMR, carbon-13-NMR, and mass spectrometry. Further, all the newly prepared molecules were assessed against their antioxidant activity. Furthermore, four compounds were assessed for their molecular docking interactions and cytotoxicity activity. The synthesized derivatives have shown moderate antioxidant activity compared to the standard BHA. The IC50 of the tilted molecules (11b, 11c, 13b, and 14b) observed for in vitro anti-cancer activities were 11.20, 15.73, 59.61, and 27.66 g/ml at 72-hour treatment time against the A549 cell lines, respectively. The tested compounds' biological evaluation showed that 11b is the most effective molecule in the series.Keywords: antioxidant activity, cytotoxicity activity, molecular docking, 1, 3, 4-Oxadiazole-2 thioether derivatives
Procedia PDF Downloads 866070 In vitro Antioxidant Activity of Derris scandens Extract
Authors: Nattawit Thiapairat
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Multiple diseases have been linked to excessive levels of free radicals, which cause tissue or cell damage as a result of oxidative stress. Many plants are sources of high antioxidant activity. Derris scandens has a high amount of phenolic and flavonoid contents which demonstrated good biological activities. This study focused on the antioxidant activity of polyphenols extracted from D. scandens. This study performs total flavonoids content and various antioxidant assays, which were 2,2-diphenyl-1-picryl-hydrazyl-hydrate (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical scavenging capacity assays. The total flavonoid content of D. scandens extract was determined and expressed as quercetin equivalents (QE)/g measured by the aluminum chloride colorimetric method. The antioxidant activity of D. scandens extract was also determined by DPPH and ABTS assays. In the DPPH assay, vitamin C was used as a positive control, whereas Trolox was used as a positive control in the ABTS assay. The half-maximal inhibitory concentration (IC50) values for D. scandens extract from DPPH and ABTS assays were 41.79 μg/mL ± 0.783 and 29.42 μg/mL ± 0.890, respectively, in the DPPH assay. To conclude, D. scandens extract consists of a high amount of total phenolic content, which exhibits a significant antioxidant activity. However, further investigation regarding antioxidant activity such as SOD, ROS, and RNS scavenging assays and in vivo experiments should be performed.Keywords: ABTS assay, antioxidant activity, Derris scandens, DPPH assays, total flavonoid content
Procedia PDF Downloads 2126069 Radiological Assessment of Fish Samples Due to Natural Radionuclides in River Yobe, North Eastern Nigeria
Authors: H. T. Abba, Abbas Baba Kura
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Assessment of natural radioactivity of some fish samples in river Yobe was conducted, using gamma spectroscopy method with NaI(TI) detector. Radioactivity is phenomenon that leads to production of radiations, whereas radiation is known to trigger or induce cancer. The fish were analyzed to estimate the radioactivity (activity) concentrations due to natural radionuclides (Radium 222(226Ra), Thorium 232 (232Th) and Potassium 40 (40K)). The obtained result show that the activity concentration for (226Ra), in all the fish samples collected ranges from 15.23±2.45 BqKg-1 to 67.39±2.13 BqKg-1 with an average value of 34.13±1.34 BqKg-1. That of 232Th, ranges from 42.66±0.81 BqKg-1 to 201.18±3.82 BqKg-1, and the average value stands at 96.01±3.82 BqKg-1. The activity concentration for 40K, ranges between 243.3±1.56 BqKg-1 to 618.2±2.81 BqKg-1 and the average is 413.92±1.7 BqKg-1. This study indicated that average daily intake due to natural activity from the fish is valued at 0.913 Bq/day, 2.577Bq/day and 11.088 Bq/day for 226Ra, 232Th and 40K respectively. This shows that the activity concentration values for fish, shows a promising result with most of the fish activity concentrations been within the acceptable limits. However locations (F02, F07 and F12) fish, became outliers with significant values of 112.53μSvy-1, 121.11μSvy-1 and 114.32μSvy-1 effective Dose. This could be attributed to variation in geological formations within the river as while as the feeding habits of these fish. The work shows that consumers of fish from River Yobe have no risk of radioactivity ingestion, even though no amount of radiation is assumed to be totally safe.Keywords: radiation, radio-activity, dose, radionuclides, river Yobe
Procedia PDF Downloads 3176068 The Influence of Physical Activity and Health Literacy on Depression Level of First and Second Turkish Generation Living in Germany
Authors: Ceren Akyüz, Ingo Froboese
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Health literacy has gained importance with the further spread of the coronavirus disease (COVID-19) worldwide and has been associated with health status in various chronic diseases. Many studies indicate that mental health can be improved by low- or moderate-intensity activity, and several studies have been proposed to explain the relationship between physical activity and mental health. The aim of the present study is to investigate the levels of physical activity, health literacy, and depression in first- and- second generation Turkish people in Germany. The research consists of 434 participants (255 females, 179 males; age 38.09 ± 13.73). 40.8 % of participants are married, and 59.2 % of participants are single. Education levels are mostly at university level (54.8 %), and graduate level is 18.9 %. While 24.9 % of the participants are second generation, 75.1 % of participants are first generation. All analyses were stratified on gender, marital status, education, generation and income status, and five age categories: 18–30, 31–40, 41–50, 51–60, and 61–79, which were defined to account for age-specific trends while maintaining sufficient cell size for statistical analysis. A correlation of depression with physical activity and health literacy levels between first- and- second generation Turks in Germany was evaluated in order to find out whether there are significant differences between the two populations and demographic variables (gender, marital status, education, generation, income status) with carrying out questionnaires which are European Health Literacy Survey Questionnaire (HLS-EU-Q47), International Physical Activity Questionnaire ( IPAQ) and the Patient Health Questionnaire-9 (PHQ-9).Keywords: health literacy, turks in germany, migrants, depression, physical activity
Procedia PDF Downloads 826067 Chemical Composition, Antioxidant and Antimicrobial Activities of the Essential Oils of Different Pinus Species from Kosovo
Authors: Fatbardhë Kurti, Giangiacomo Beretta, Behxhet Mustafa, Fabrizio Gelmini, Avni Hajdari
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Chemical profile, antioxidant and antimicrobial activity of total and fractionated essential oils (EOs) (F1 – hexane, F2 – hexane/diethyl ether, F3 – diethyl ether) derived from five Pinus species (Pinus heldreichii, P. peuce, P. mugo, Pinus nigra, P. sylvestris), were investigated. The hydrodistilled EOs and their chromatographic fractions (direct solid phase extraction, SPE) were analysed by GC-MS and 112 compounds separated and identified. The main constituents were α-pinene, β-pinene, D-limonene, β-caryophyllene, germacrene D, bornyl acetate and 3-carene. The antioxidant activities of total EOs were lower than those of the corresponding fractions, with F2 the strongest in all cases. EOs and fractions showed different degrees of antibacterial efficacy against different microbial pathogens (moderately strong antimicrobial activity against C. albicans and C. krusei ,while low or no activity against E. faecalis and E. coli strains). The detected inhibition zones and MICs for the EOs and fractions were in the range of 14 -35 mm and 0.125 - 1% (v/v), respectively. The components responsible for the antioxidant and antimicrobial activity were oxygenated monoterpenes and sesquiterpenes recovered in the polar EO fractions. These activities seem to be regulated by reciprocal interactions among the different subclasses of phytochemical species present in the EOs.Keywords: antagonism, antioxidant activity, antibacterial activity, essential oil, fractions, GC-MS, pinus
Procedia PDF Downloads 2306066 Study on the Relationship between the Emission Property of Barium-Tungsten Cathode and Micro-Area Activity
Authors: Zhen Qin, Yufei Peng, Jianbei Li, Jidong Long
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In order to study the activity of the coated aluminate barium-tungsten cathodes during activation, aging, poisoning and long-term use. Through a set of hot-cathode micro-area emission uniformity study device, we tested the micro-area emission performance of the cathode under different conditions. The change of activity of cathode micro-area was obtained. The influence of micro-area activity on the performance of the cathode was explained by the ageing model of barium-tungsten cathode. This helps to improve the design and process of the cathode and can point the way in finding the factors that affect life in the cathode operation.Keywords: barium-tungsten cathode, ageing model, micro-area emission, emission uniformity
Procedia PDF Downloads 4076065 Synthesis of Quinazoline Derivatives as Selective Inhibitors of Cyclooxygenase-1 Enzyme
Authors: Marcela Dvorakova, Lenka Langhansova, Premysl Landa
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A series of quinazoline derivatives bearing aromatic rings in 2- and 4-positions were prepared and tested for their biological activity. Firstly, the compounds were evaluated for their potential to inhibit various kinases, such as autophagy activating kinase ULK1, 3-Phosphoinositide-dependent kinase 1, and TANK-binding kinase 1. None of the compounds displayed any activity on these kinases. Secondly, the compounds were tested for their anti-inflammatory activity expressed as cyclooxygenase (COX) isoforms and 5-lipoxygenase (5-LOX) inhibition. Three of the compounds showed significant selectivity towards COX-1 isoform (COX-2/COX-1 SI = 20-30). They inhibited COX-1 in a single-digit µM range. There was also one compound that exhibited inhibitory activity towards all three tested enzymes in µM range (IC50COX-1 = 1.9 µM; IC50COX-2 and 5-LOX = 10.1µM. COX-1 inhibition was until recently considered undesirable due to COX-1 constitutive expression in most cell types and tissues. Thus, there are not many compounds known with selective COX-1 activity. However, it is now believed that COX-1 plays an important role in the pathophysiology of several acute and chronic disorders, including cancer or neurodegenerative diseases. Thus, the discovery of effective COX-1 selective inhibitors is desirable and important.Keywords: cyclooxygenases, kinases, lipoxygenases, quinazolines
Procedia PDF Downloads 1336064 The Formation of Motivational Sphere for Learning Activity under Conditions of Change of One of Its Leading Components
Authors: M. Rodionov, Z. Dedovets
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This article discusses ways to implement a differentiated approach to developing academic motivation for mathematical studies which relies on defining the primary structural characteristics of motivation. The following characteristics are considered: features of realization of cognitive activity, meaning-making characteristics, level of generalization and consistency of knowledge acquired by personal experience. The assessment of the present level of individual student understanding of each component of academic motivation is the basis for defining the relevant educational strategy for its further development.Keywords: learning activity, mathematics, motivation, student
Procedia PDF Downloads 4156063 Leisure, Domestic or Professional Activities so as to Prevent Cognitive Decline: Results FreLE Longitudinal Study
Authors: Caroline Dupre, David Hupin, Christ Goumou, Francois Belan, Frederic Roche, Thomas Celarier, Bienvenu Bongue
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Background: Previous cohorts have been notably criticized for not studying the different type of physical activity and not investigating household activities. The objective of this work was to analyse the relationship between physical activity and cognitive decline in older people living in the community. Impact of type of physical activity on the results has been realised. Methods: The study used data from the longitudinal and observational study , FrèLE (FRagility: Longitudinal Study of Expressions). The collected data included: socio-demographic variables, lifestyle, and health status (frailty, comorbidities, cognitive status, depression). Cognitive decline was assessed by using: Mini-Mental State Examination (MMSE) and Montreal Cognitive Assessment (MoCA). Physical activity was assessed by the Physical Activity Scale for the Elderly (PASE). This tool is structured in three sections: the leisure activity, domestic activity, and professional activity. Logistic regressions and proportional hazards regression models (Cox) were used to estimate the risk of cognitive disorders. Results: At baseline, the prevalence of cognitive disorders was 6.9% according to MMSE. In total, 1167 participants without cognitive disorders were included in the analysis. The mean age was 77.4 years, and 52.1% of the participants were women. After a 2 years long follow-up, we found cognitive disorders on 53 participants (4.5%). Physical activity at baseline is lower in older adults for whom cognitive decline was observed after two years of follow-up. Subclass analyses showed that leisure and domestic activities were associated with cognitive decline, but not professional activities. Conclusions: Analysis showed a relationship between cognitive disorders and type of physical activity. The current study will be completed by the MoCA for mild cognitive impairment. These findings compared to other ongoing studies, will contribute to the debate on the beneficial effects of physical activity on cognition.Keywords: aging, cognitive function, physical activity, mixed models
Procedia PDF Downloads 1266062 Optimised Path Recommendation for a Real Time Process
Authors: Likewin Thomas, M. V. Manoj Kumar, B. Annappa
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Traditional execution process follows the path of execution drawn by the process analyst without observing the behaviour of resource and other real-time constraints. Identifying process model, predicting the behaviour of resource and recommending the optimal path of execution for a real time process is challenging. The proposed AlfyMiner: αyM iner gives a new dimension in process execution with the novel techniques Process Model Analyser: PMAMiner and Resource behaviour Analyser: RBAMiner for recommending the probable path of execution. PMAMiner discovers next probable activity for currently executing activity in an online process using variant matching technique to identify the set of next probable activity, among which the next probable activity is discovered using decision tree model. RBAMiner identifies the resource suitable for performing the discovered next probable activity and observe the behaviour based on; load and performance using polynomial regression model, and waiting time using queueing theory. Based on the observed behaviour αyM iner recommend the probable path of execution with; next probable activity and the best suitable resource for performing it. Experiments were conducted on process logs of CoSeLoG Project1 and 72% of accuracy is obtained in identifying and recommending next probable activity and the efficiency of resource performance was optimised by 59% by decreasing their load.Keywords: cross-organization process mining, process behaviour, path of execution, polynomial regression model
Procedia PDF Downloads 3336061 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 1566060 Critical Activity Effect on Project Duration in Precedence Diagram Method
Authors: Salman Ali Nisar, Koshi Suzuki
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Precedence Diagram Method (PDM) with its additional relationships i.e., start-to-start, finish-to-finish, and start-to-finish, between activities provides more flexible schedule than traditional Critical Path Method (CPM). But, changing the duration of critical activities in PDM network will have anomalous effect on critical path. Researchers have proposed some classification of critical activity effects. In this paper, we do further study on classifications of critical activity effect and provide more information in detailed. Furthermore, we determine the maximum amount of time for each class of critical activity effect by which the project managers can control the dynamic feature (shortening/lengthening) of critical activities and project duration more efficiently.Keywords: construction project management, critical path method, project scheduling, precedence diagram method
Procedia PDF Downloads 5106059 Smartphone-Based Human Activity Recognition by Machine Learning Methods
Authors: Yanting Cao, Kazumitsu Nawata
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As smartphones upgrading, their software and hardware are getting smarter, so the smartphone-based human activity recognition will be described as more refined, complex, and detailed. In this context, we analyzed a set of experimental data obtained by observing and measuring 30 volunteers with six activities of daily living (ADL). Due to the large sample size, especially a 561-feature vector with time and frequency domain variables, cleaning these intractable features and training a proper model becomes extremely challenging. After a series of feature selection and parameters adjustment, a well-performed SVM classifier has been trained.Keywords: smart sensors, human activity recognition, artificial intelligence, SVM
Procedia PDF Downloads 1416058 Implementing Activity-Based Costing in Architectural Aluminum Projects: Case Study and Lessons Learned
Authors: Amer Momani, Tarek Al-Hawari, Abdallah Alakayleh
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This study explains how to construct an actionable activity-based costing and management system to accurately track and account the total costs of architectural aluminum projects. Two ABC models were proposed to accomplish this purpose. First, the learning and development model was introduced to examine how to apply an ABC model in an architectural aluminum firm for the first time and to be familiar with ABC concepts. Second, an actual ABC model was built on the basis of the results of the previous model to accurately trace the actual costs incurred on each project in a year, and to be able to provide a quote with the best trade-off between competitiveness and profitability. The validity of the proposed model was verified on a local architectural aluminum company.Keywords: activity-based costing, activity-based management, construction, architectural aluminum
Procedia PDF Downloads 1016057 Synthesis of 3,4-Dihydro-1H-Quinoxalin-2-Ones and 1H‑Quinolin-2-Ones and Evaluation of Their Anti-Bacterial Activity
Authors: Ali Amiri, Arash Esfandiari, Elham Zarenezhad
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We report here an efficient and rapid method for the preparation of 3,4-dihydro-1H-quinoxalin-2-ones and 1H‑quinolin-2-ones that involves grinding of o-, m-, or p‑phenylenediamine and three dialkyl acetylenedicarboxylates using a pestle and mortar. This solvent-free approach requires only a few minutes of reaction time. This type of reaction is expected to be the most economical method since neither catalyst nor solvent is used. Finally, all synthesised compounds were screened for antimicrobial activity against two Gram-positive bacteria (Pseudomonas aeruginosa PTCC 1077, Escherichia coli PTCC1330) and two Gram-negative bacteria (Staphylococcus aureus PTCC 1133, Bacillus cereus PTCC 1015) and their activity. Compared with gentamycin and ampicillin as reference drugs for Gram-negative and Gram-positive bacteria, respectively. The minimum inhibitory concentration (MIC) of the synthesised compounds and reference drugs were determined by the microdilution method. Good antibacterial activity was observed for 3,4-dihydro-1H-quinoxalin-2-ones against all species of Gram-positive and Gram-negative bacteria, and1H‑quinolin-2-ones showed good antibacterial activity against two Gram-positive bacteria.Keywords: quinolin, quinoxalin, anti-bacterial activity, minimum inhibitory concentration (MIC)
Procedia PDF Downloads 3346056 Determination of Antimicrobial Effect and Essential Oil Composition Salvia verticillata L. Subsp. amasiaca
Authors: Tanju Teker, Yener Tekeli̇, Esra Karpuz
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Salvia species are known as medicinal plant and often used in public. The antimicrobial effects and essential oil composition of Salvia verticillata L. subsp. amasiaca were determined. The antimicrobial activity is determined by using disk diffusion method against two Gram-positive bacteria, two Gram-negative bacteria and one kind of yeast and essential oil composition was determined by GC - MS. As a result of antimicrobial analysis while sample has shown very strong antimicrobial activity against Staphylococcus aureus, moderately effective against Pseudomonas aeruginosa and low effective against Enterococcus faecalis, it has not shown antimicrobial activity against Escherichia coli and C. albicans. Trans-caryophyllene (% 35.07), germacrene-d (% 10.98) and caryopyllene oxide (% 5.81) are the main components of essential oil composition.Keywords: salvia, medicinal plant, antimicrobial activity, essential oil
Procedia PDF Downloads 4546055 Evaluation of Mutagenic and Antimutagenic Activities of Some Biological Active Benzoxazoles in the Ames Test
Authors: Özlem Arpacı, Zeliha Soysal, Nuran Diril
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Benzoxazoles are heterocyclic compounds that have a fused benzene and an oxazole ring. These heterocyclic compounds are reported to have antibacterial, antitubercular, antifungal, antiviral, antioxidant and anticancer activities. In this study, some benzoxazole derivatives that have broad antimicrobial and potent antitumoral activities, are investigated their mutagenic activities with using the Ames Test. The Ames test was conducted using Salmonella typhimurium TA98, TA100 and TA102 tester strains in the standard plate incorporation assay in the absence of liver S9 fraction. The results are evaluated using SPSS and none of the benzoxazole derivatives showed mutagenic activity using the Ames test in the absence of S9 liver fraction.Keywords: benzoxazoles, ames test, mutagenic activity, antimutagenic activity, antitumoral activity
Procedia PDF Downloads 3456054 Impact of Education on Levels of Physical Activity and Depression in Taiwanese Vegetarians and Omnivores
Authors: Ya-Lin Chang, Chia Chen Chang, Yu-Ru Liang, Joyce Chen, You-Kang Chang, Tina Chiu
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Physical activity and mental health status are important for health. The purpose of this study was to examine levels of physical activities and depression in Taiwanese vegetarians (VEG) and omnivores (OMNI). Sixty-three vegetarians (20 males) and 56 omnivores (23 males) with an average age of 51 years were recruited for a food frequency validation study at Taipei Tzu Chi Hospital from July to September in 2016. Participants filled out a validated Chinese version international physical activity questionnaire-short-form (IPAQ), Beck Depression Inventory-II-Chinese version (BDI), food frequency questionnaire (FFQ) and a questionnaire on demographics and medical history upon recruitment. Total BDI scores were calculated for depression and the metabolic equivalent of task (MET) was calculated for physical activity levels. Mann-Whitney U tests and Chi-square test were used to compare demographics, physical activity levels and depression scores. VEG and OMNI did not differ significantly on MET (1441.9 ± 3387.3 vs. 1605.8 ± 2486.1. p=0.2652, respectively). VEG scored slightly lower on BDI compared to OMNI without statistical significance (5.6 ± 5.7 vs. 7.4 ± 6.3. p=0.06). In addition, we found that regardless of diet practice, those who held a college degree and above scored better on MET (1788.1 ± 2532.6 vs. 1215.5 ± 3425.5. p=0.0014) and BDI (5.2 ± 5.1 vs. 7.8 ± 6.7. p=0.03). In this cross-sectional study, Taiwanese vegetarians and omnivores scored comparatively on physical activity levels and depression. However, education is a significant determinant of physical activity and depression.Keywords: BDI, diet, education, physical activity
Procedia PDF Downloads 3886053 Methyltrioctylammonium Chloride as a Separation Solvent for Binary Mixtures: Evaluation Based on Experimental Activity Coefficients
Authors: B. Kabane, G. G. Redhi
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An ammonium based ionic liquid (methyltrioctylammonium chloride) [N8 8 8 1] [Cl] was investigated as an extraction potential solvent for volatile organic solvents (in this regard, solutes), which includes alkenes, alkanes, ketones, alkynes, aromatic hydrocarbons, tetrahydrofuran (THF), alcohols, thiophene, water and acetonitrile based on the experimental activity coefficients at infinite THF measurements were conducted by the use of gas-liquid chromatography at four different temperatures (313.15 to 343.15) K. Experimental data of activity coefficients obtained across the examined temperatures were used in order to calculate the physicochemical properties at infinite dilution such as partial molar excess enthalpy, Gibbs free energy and entropy term. Capacity and selectivity data for selected petrochemical extraction problems (heptane/thiophene, heptane/benzene, cyclohaxane/cyclohexene, hexane/toluene, hexane/hexene) were computed from activity coefficients data and compared to the literature values with other ionic liquids. Evaluation of activity coefficients at infinite dilution expands the knowledge and provides a good understanding related to the interactions between the ionic liquid and the investigated compounds.Keywords: separation, activity coefficients, methyltrioctylammonium chloride, ionic liquid, capacity
Procedia PDF Downloads 1436052 Detection of Telomerase Activity as Cancer Biomarker Using Nanogap-Rich Au Nanowire SERS Sensor
Authors: G. Eom, H. Kim, A. Hwang, T. Kang, B. Kim
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Telomerase activity is overexpressed in over 85% of human cancers while suppressed in normal somatic cells. Telomerase has been attracted as a universal cancer biomarker. Therefore, the development of effective telomerase activity detection methods is urgently demanded in cancer diagnosis and therapy. Herein, we report a nanogap-rich Au nanowire (NW) surface-enhanced Raman scattering (SERS) sensor for detection of human telomerase activity. The nanogap-rich Au NW SERS sensors were prepared simply by uniformly depositing nanoparticles (NPs) on single-crystalline Au NWs. We measured SERS spectra of methylene blue (MB) from 60 different nanogap-rich Au NWs and obtained the relative standard deviation (RSD) of 4.80%, confirming the superb reproducibility of nanogap-rich Au NW SERS sensors. The nanogap-rich Au NW SERS sensors enable us to detect telomerase activity in 0.2 cancer cells/mL. Furthermore, telomerase activity is detectable in 7 different cancer cell lines whereas undetectable in normal cell lines, which suggest the potential applicability of nanogap-rich Au NW SERS sensor in cancer diagnosis. We expect that the present nanogap-rich Au NW SERS sensor can be useful in biomedical applications including a diverse biomarker sensing.Keywords: cancer biomarker, nanowires, surface-enhanced Raman scattering, telomerase
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