Search results for: xanthine oxidase inhibitory activity

Authors: Tomasz Frączek, Agata Paneth, Rafał Kamiński, Agnieszka Krakowiak, Piotr Paneth

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Azoles are a promising class of the new generation of HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs). From thousands of reported compounds, many possess the same basic structure of an aryl substituted azole ring linked by a thioglycolamide chain with another aromatic ring. To find novel extensions for this primary scaffold, we explored the 5-position substitution of triazole NNRTIs using molecular docking followed by synthesis of selected compounds. We discovered that heterocyclic substituents in 5-position of the triazole ring are detrimental to the inhibitory activity of compounds with 4-membered thioglycolamide linker. This substitution seems to be viable only for compounds with a shorter 2-membered linker such as in derivatives of 4‐benzyl‐3‐(benzyl-sulfanyl)‐5‐(thiophen‐2‐yl)‐4H‐1,2,4‐triazole reported earlier. A new scaffold of 2‐[(4‐benzyl‐5‐methyl‐4H‐1,2,4‐triazol‐3‐yl)sulfanyl]‐N‐phenylacetamide has been identified in this study.

Keywords: docking, molecular modeling, drug design, novel scaffolds

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Authors: Kuan Yin Hsiao, Shyh Ming Kuo, Yi Jhen Wu, Chin Wen Chuang, Chuen-Fu Lin, Wei-qing Yang, Han Hsiang Huang

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Anti-tumor effects of natural products, like compounds from marine sponges and soft corals, have been investigated for decades. Polymeric nanoparticles prepared from biodegradable and biocompatible molecules, such as Hyaluronan (HA), Chitosan (CHI) and gelatin have been widely studied. Encapsulation of anti-cancer therapies by the biopolymeric nanoparticles in drug delivery system is potentially capable of improving the therapeutic effects and attenuating their toxicity. In the current study, the anti-bladder cancer effects of heteronemin extracted from the sponge Hippospongia sp. with or without HA and CHI nanoparticle encapsulation were assessed and evaluated in vitro. Results showed that IC50 (half maximal inhibitory concentration) of heteronemin toward T24 human bladder cancer cell viability is approximately 0.18 µg/mL. Both plain and HA nanoparticles-encapsulated heteronemin at 0.2 and 0.4 µg/mL significantly reduced T24 cell viability (P<0.001) while HA nanoparticles-encapsulated heteronemin showed weaker viability-inhibitory effects on L929 fibroblasts compared with plain heteronemin at the identical concentrations. HA and CHI nanoparticles-encapsulated heteronemin exhibited significantly stronger inhibitory effects against migration of T24 human bladder cancer cell than those exerted by plain heteronemin at the same concentrations (P<0.001). The flow cytometric results showed that 0.2 µg/mL HA and CHI nanoparticles-encapsulated heteronemin induced higher early apoptosis rate than that induced by plain heteronemin at the same concentration. These results show that HA and CHI nanoparticle encapsulation is able to elevate anti-migratory and apoptosis-inducing effects exerted by heteronemin against bladder cancer cells in vitro. The in vivo anti-bladder cancer effects of the compound with or without HA/CHI nanoparticle encapsulation will be further investigated and examined using murine tumor models. The data obtained from this study will extensively evaluate of the anti-bladder cancer effects of heteronemin as well as HA/CHI-encapsulated heteronemin and pave a way to develop potential bladder cancer treatment.

Keywords: heteronemin, nanoparticles, hyaluronan, chitosan, bladder cancer

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Authors: Hairin Taha, P. Narrima, M. A. Hapipah, A. M. Mustafa

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The chemical constituents and antioxidant activity of the leaf essential oils of Pseuduvaria monticola and Pseuduvaria macrophylla from the Annonaceae family were investigated. GC-TOFMS analyses identified 46 compounds from Pseuduvaria monticola and 11 compounds from Pseuduvaria macrophylla. The major constituents in the leaf essential oil of Pseuduvaria monticola were a-cadinol (13.0%), calamenene-cis (6.9%), alfa copaene (4%), and epizonarene (3.8%), while in the leaf essential oil of Pseuduvaria macrophylla were caryophyllene oxide (29.7%) and elimicin (28%). The antioxidant activity of both the essential oils were determined using the 2,2'-diphenyl-1-picrylhydrazyl assay (DPPH). The present study suggests that both essential oils demonstrated good antioxidant activity.

Keywords: Pseuduvaria monticola, Pseuduvaria macrophylla, leaf essential oils, GC-MSTOF, antioxidant activity

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Authors: Mohammadjavad Sotoudeheian, Navid Farahmandian

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Kawasaki disease (KD) is the primary cause of acquired pediatric heart disease as an acute vasculitis. In children with prolonged fever, rash, and inflammation of the mucosa KD must be considered as a clinical diagnosis. There is a persuasive suggestion of immune-mediated damage as the pathophysiologic cascade of KD. For example, the invasion of cytotoxic T-cells supports a viral etiology and the inflammasome of the innate immune system is a critical component in the vasculitis formation in KD. Animal models of KD propose the cytokine profiles, such as increased IL-1 and GM-CSF, which cause vascular damage. CRP and IFN-γ elevated expression and the upregulation of IL-6, and IL-10 production are also described in previous studies. Untreated KD is a critical risk factor for coronary artery diseases and myocardial infarction. Vascular damage may encompass amplified T-cell activity. SMAD3 is an essential molecule in down-regulating T-cells and increasing expression of FoxP3. It has a critical effect in the differentiation of regulatory T-cells. The discrepancy of regulatory T-cells and pro-inflammatory Th17 has been studied in acute coronary syndrome during KD. However in the coronary artery damaged lymphocytes and IgA plasma cells are seen at the lesion locations, the major immune cells in the coronary lesions are monocytes/macrophages and neutrophils. These cells secrete TNF-α, and activates matrix metalloprotease (MMP)-9, reducing the integrity of vessels and prompting patients to arise aneurysm. MMPs can break down the components of the extracellular matrix and assist immune cell movement. IVIG as an effective form of treatment clarified the role of the immune system, which may target pathogenic antigens and regulate cytokine production. Several reports have revealed that in the coronary arteries, high expression of MMP-9 in monocyte/macrophage results in pathologic cascades. Curcumin is a potent antioxidant and anti-inflammatory molecule. Curcumin decreases the production of reactive oxygen and nitrogen species and inhibits transcription factors like AP-1 and NF-κB. Curcumin also contains the characteristics of inhibitory effects on MMPs, especially MMP-9. The upregulation of MMP-9 is an important cellular response. Curcumin treatment caused a reverse effect and down-regulates MMP-9 gene expression which may fund the anti-inflammatory effect. Curcumin inhibits MMP-9 expression via PKC and AMPK-dependent pathways in Human monocytes cells. Elevated expression and activity of MMP-9 are correlated with advanced vascular lesions. AMPK controls lipid metabolism and oxidation, and protein synthesis. AMPK is also necessary for the MMP-9 activity and THP-1 cell adhesion to endothelial cells. Curcumin was shown to inhibit the activation of AMPKα. Compound C (AMPK inhibitor) inhibits MMP-9 expression level. Therefore, through inactivating AMPKs and PKC, curcumin decreases the MMP-9 level, which results in inhibiting monocyte/macrophage differentiation. Compound C also suppress the phosphorylation of three major classes of MAP kinase signaling, suggesting that curcumin may suppress MMP-9 level by inactivation of MAPK pathways. MAPK cascades are activated to induce the expression of MMP-9. Curcumin inhibits MAPKs phosphorylation, which contributes to the down-regulation of MMP-9. This study demonstrated that the potential inhibitory properties of curcumin over MMP-9 lead to a therapeutic strategy to reduce the risk of coronary artery involvement during KD.

Keywords: MMP-9, coronary artery aneurysm, Kawasaki’s disease, curcumin, AMPK, immune system, NF-κB, MAPK

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Authors: Kamta P. Namdeo

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Novel thiazolidino-(3,2-b)-1, 2,4-triazole-5(6H)-one derivatives were synthesized, and anticancer activity was studied on human breast cancer cell line MFC7. It showed a significant decrease in cell viability with reference to the standard. The findings suggest that nitro-substituted compound showed best anticancer activity and activity was due to the triazole and thiazolidinone hetero nucleus present in the structure.

Keywords: anti-cancer, adriamycine, thiazolidinone, 1, 2, 4-triazole, thiazolidino-triazolone

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Authors: Andreia Guimaraes Farnese, Mateus Fernandes Reu Urban, Leandro Procopio, Renato Zangaro, Regiane Albertini

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Senescence changes include postural balance, inferring the risk of falls, and can lead to fractures, bedridden, and the risk of death. Physical activity, e.g., cardiovascular exercises, is notable for improving balance due to brain cell stimulations, but fine coordination exercises also elevate cell brain metabolism. This study aimed to verify whether the elderly person who performs fine motor activity has a balance similar to that of those who practice physical activity. The subjects were divided into three groups according to the activity practice: control group (CG) with seven participants for the sedentary individuals, motor coordination group (MCG) with six participants, and activity practitioner group (PAG) with eight participants. Data comparisons were from the Berg balance scale, Time up and Go test, and stabilometric analysis. Descriptive statistical and ANOVA analyses were performed for data analysis. The results reveal that including fine motor activities can improve the balance of the elderly and indirectly decrease the risk of falls.

Keywords: balance, barapodometer, coordination, elderly

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Authors: Cheyma Bensaci, Mokhtar Saidi, Zineb Ghiaba

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The first objective of this study is to determine the phenolic contents and antioxidant capacities of three different varieties of date palm (Phoenix dactylifera L.) fruit (DPF) from Algeria were using three different solvents. As for the second objective is to find the correlation of phenolic contents with the both DPPH radical scavenging and reducing power activity. These results showed that date had strongly scavenging activity on DPPH .The IC50 value for DPPH radical scavenging activity was 0.15 mg/ml in acetone/H2O extract from Gh. And also, acetone/H2O extract from Gh showed the best AEAC value for reducing power was 8,48 mM. The results also showed that there are a positive correlation, so confined values between 0.153 and 0.972.

Keywords: phoenix dactylifera, antioxidant activity, correlation, reducing power

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Authors: Luai Z. Hasoun, Steven W. Bailey, Kitti K. Outlaw, June E. Ayling

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Human skin color is thought to have evolved to balance sufficient photochemical synthesis of vitamin D versus the need to protect not only DNA but also folate from degradation by ultraviolet light (UV). Although the risk of DNA damage and subsequent skin cancer is related to light skin color, the effect of UV on skin folate of any species is unknown. Here we show that UVA irradiation at 13 mW/cm2 for a total exposure of 187 J/cm2 (similar to a maximal daily equatorial dose) induced a significant loss of total folate in epidermis of ex vivo white skin. No loss was observed in black skin samples, or in the dermis of either color. Interestingly, while the concentration of 5 methyltetrahydrofolate (5-MTHF) fell in white epidermis, a concomitant increase of tetrahydrofolic acid was found, though not enough to maintain the total pool. These results demonstrate that UVA indeed not only decreases folate in skin, but also rearranges the pool components. This could be due in part to the reported increase of NADPH oxidase activity upon UV irradiation, which in turn depletes the NADPH needed for 5-MTHF biosynthesis by 5,10-methylenetetrahydrofolate reductase. The increased tetrahydrofolic acid might further support production of the nucleotide bases needed for DNA repair. However, total folate was lost at a rate that could, with strong or continuous enough exposure to ultraviolet radiation, substantially deplete light colored skin locally, and also put pressure on total body stores for individuals with low intake of folate.

Keywords: depletion, folate, human skin, ultraviolet

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Authors: J. M. Hung, J. S. Chan, M. I. Kuo, D. S. Chan, C. P. Lu

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Wheat germ is a by-product obtained from wheat milling and it contains highly concentrated nutrients. Due to highly lipase and lipoxygenase activities, wheat germ products can easily turn into rancid flavor and cause a short life. The objective of this study is to control moisture content and retard lipid hydrolysis by fluidized-bed drying. The raw wheat germ of 2 kg was dried with a vertical batch fluidized bed with the following varying conditions, inlet air temperature of 50, 80 and 120°C, inlet air velocity of 3.62 m/s. The experiment was designed to obtain a final product at around 40°C with water activity of 0.3 ± 0.1. Changes in the moisture content, water activity, enzyme activity of dried wheat germ during storage were measured. Results showed the fluidized-bed drying was found to reduce moisture content, water activity and lipase activity of raw wheat germ. After drying wheat germ, moisture content and water activity were between 5.8% to 7.2% and 0.28 to 0.40 respectively during 12 weeks of storage. The variation range of water activity indicated to retard lipid oxidation. All drying treatments displayed inactivation of lipase, except for drying condition of 50°C which showed relative high enzyme activity. During storage, lipase activity increased slowly during the first 6 weeks of storage and reached a plateau for another 6 weeks. As a result, using a fluidized-bed dryer was found to be effective drying technique in improving storage stability of wheat germ.

Keywords: wheat germ, fluidized-bed dryer, storage, lipase, stability

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Authors: Fakhreia A. Al Sagheer, Enas I. Ibrahim, Khaled D. Khalil

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N-Acryloyl morpholine, NAM, was grafted onto chitosan utilizing homogeneous conditions with 1% acetic acid as the solvent, and potassium persulfate and sodium sulfite as the redox initiator. The effects of various reaction parameters, such as time, temperature, and monomer and initiator concentrations, on the percentage of grafting (G%) and the grafting efficiency (E%) were determined. The graft copolymer showed a remarkably improved crystallinity, as compared to the unmodified chitosan, based on the FESEM, XRD, and DSC results. Chitosan-g-poly(N-acryloyl morpholine) (Cs-PNAM), the copolymer obtained by using this procedure, was characterized by utilizing FTIR, FESEM, TGA, and XRD analysis. As expected, the results of an evaluation of antibacterial and antifungal activities show that the grafted chitosan copolymers exhibit stronger inhibitory effects against both types of microbes than does chitosan. Moreover, the size of the inhibition zone created by the graft copolymer was observed to be proportional to its G% corresponding to its morpholine content. Fortunately, the graft copolymer showed a marked growth inhibition against candidiasis (C.Albicans and C.Kefyr). We conclude that the graft copolymer may be highly effective in the prevention and treatment of candidiasis. In addition, the extent and pH dependence of uptake of different types of dyes (acidic: EBT, and MV; and basic: MB) by grafted chitosan in pH 6.5 aqueous solutions was determined. The results show that, the grafted copolymer exhibited a greater affinity to absorb the acid dyes more than the basic ones especially at relatively low temperature. Thus the modified chitosan can be used, in wastewater treatment, as efficient economic absorbent especially for anionic dyes from the industrial processing effluents.

Keywords: chitosan, N-Acryloyl morpholine, homogeneous grafting, antimicrobial activity, dye uptake

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Authors: Tania Mannan, Rahelee Zinnat, Fatema Jebunnesa, Israt Ara Hossain

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Background: Exposure to arsenic has known toxic effects but the effect on pregnancy outcomes is not as widely documented especially in women with diabetes. Growing evidence has suggested a potential role of arsenic exposure in the development of gestational diabetes mellitus (GDM). Therefore, we aimed to investigate the association of urinary arsenic (UAs) with birth outcomes in GDM subjects. Methods: Under an observational cross-sectional design a total of 263 GDM subjects (age in years, M±SD, 21±3.7) residing in an arsenic affected area of Bangladesh, were subjected to a 2 sample OGTT at the third trimester of gestation. Among them, 73 GDM and 190 non-GDM subjects enrolled in this study. Clinical and anthropometric measurements were done by standard techniques. Degree of chronic arsenic exposure was assessed by the level of UAs level. According to World Health Organization (WHO) criteria, GDM was diagnosed and neonatal outcomes using APGAR (Activity Pulse Grimace Appearance Respirations) Score, birth weight and size were assessed by a specialist obstetrician. Serum glucose was measured by the Glucose Oxidase method and UAs level was determined by ultraviolet/visible spectrophotometry. Result: Out of the 263 pregnant women, 28% developed GDM. Urinary Arsenic was significantly higher in the GDM as compared to the non-GDM group [UAs, µg/l, M±SD (range), 204.2±67.0 (67.0-377.0) vs 77.3±38.1 (22.0-99.0), p < 0.001]. Activity Pulse Grimace Appearance Respirations Score of the neonates from GDM mothers was significantly lower compared to the neonates from non-GDM mothers [APGAR Score, M±SD, 4.7±0.8 vs. 6.4±0.7, p<0.001]. Pearson’s correlation analysis in GDM subjects revealed that UA levels were found to have a significant positive correlation with both fasting and postprandial serum glucose levels (p < 0.001) and (p < 0.001) respectively. Again, a significant inverse correlation of UAs with birth weight and size was observed (p < 0.001). The APGAR Score of the neonates were found to have a significant negative correlation (p < 0.001) with UAs level. Conclusion: The effect of chronic arsenic exposure is associated with glucose intolerance during pregnancy and it also adversely affects birth outcomes. The study suggests further research on the impact of total arsenic exposure on pregnancy outcomes.

Keywords: APGAR score, arsenic exposure, birth outcome, gestational diabetes mellitus,

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Authors: Rashmi Gupta

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It is unclear whether arousal or valence modulates the response inhibition process. It has been suggested that irrelevant positive emotional information (e.g., happy faces) and negative emotional information (e.g., angry faces) interact with attention differently. In the present study, we used arousal-matched irrelevant happy and angry faces. These faces were used as stop-signals in the stop-signal paradigm. There were two kinds of trials: go-trials and stop-trials. Participants were required to discriminate between the letter X or O by pressing the corresponding keys on go-trials. However, a stop signal was occasionally presented on stop trials, where participants were required to withhold their motor response. A significant main effect of emotion on response inhibition was observed. It indicated that the valence of a stop signal modulates inhibitory control. We found that stop-signal reaction time was faster in response to irrelevant angry faces than happy faces, indicating that irrelevant angry faces facilitate the response inhibition process compared to happy faces. These results shed light on the interaction of emotion with cognitive control functions.

Keywords: attention, emotion, response inhibition, inhibitory control

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Authors: Supatra Karnjanapratum, Soottawat Benjakul

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Gelatin hydrolysate, especially from marine resource, has been known to possess antioxidative activity. Nevertheless, the activity is still lower in comparison with the commercially available antioxidant. Maillard reactions can be use to increase antioxidative activity of gelatin hydrolysate, in which the numerous amino group could be involved in glycation. In the present study, gelatin hydrolysate (GH) from unicorn leatherjacket skin prepared using glycyl endopeptidase with prior autolysis assisted process was used for preparation of Maillard reaction products (MRPs) under dry condition. The impacts of different factors including, types of saccharides, GH to saccharide ratio, incubation temperatures, relative humidity (RH) and times on antioxidative activity of MRPs were investigated. MRPs prepared using the mixture of GH and galactose showed the highest antioxidative activity as determined by both ABTS radical scavenging activity and ferric reducing antioxidant power during heating (0-48 h) at 60 °C with 65% RH, compared with those derived from other saccharide tested. GH to galactose ratio at 2:1 (w/w) yielded the MRPs with the highest antioxidative activity, followed by the ratios of 1:1 and 1:2, respectively. When the effects of incubation temperatures (50, 60, 70 °C) and RH (55, 65, 75%) were examined, the highest browning index and the absorbance at 280 nm were found at 70 °C, regardless of RH. The pH and free amino group content of MRPs were decreased with the concomitant increase in antioxidative activity as the reaction time increased. Antioxidative activity of MRPs generally increased with increasing temperature and the highest antioxidative activity was found when RH of 55% was used. Based on electrophoresis of MRP, the polymerization along with the formation of high molecular weight material was observed. The optimal condition for preparing antioxidative MRPs was heating the mixture of GH and galactose (2:1) at 70 °C and 55% RH for 36 h. Therefore, antioxidative activity of GH was improved by Maillard reaction and the resulting MRP could be used as natural antioxidant in food products.

Keywords: antioxidative activity, gelatin hydrolysate, maillard reaction, unicorn leatherjacket

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Authors: Abhijit Das, Runu Chakraborty

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Tea is the most widely consumed beverage aside from water; it is grown in about 30 countries with a per capita worldwide consumption of approximately 0.12 liter per year. Green tea is of growing importance with its antioxidant contents associated with its health benefits. The various extraction methods can influence the polyphenol concentrations of green tea. The purpose of the study was to quantify the polyphenols, flavonoid and antioxidant activity of both caffeinated and decaffeinated form of tea manufactured commercially in Assam, North Eastern part of India. The results display that phenolic/flavonoid content well correlated with antioxidant activity which was performed by DPPH (2,2-diphenyl-1-picrylhydrazyl) and FRAP (Ferric reducing ability of plasma) assay. After decaffeination there is a decrease in the polyphenols concentration which also affects the antioxidant activity of green tea. For the enrichment of antioxidant activity of decaffeinated tea a herbal plant extract is used which shows a synergistic effect between green tea and herbal plant phenolic compounds.

Keywords: antioxidant activity, decaffeination, green tea, flavonoid content, phenolic content, plant extract

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Authors: Maria Medrano, Cristina Cadenas-Sanchez, Maddi Oses, Lide Arenaza, Maria Amasene, Idoia Labayen

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The COVID-19 outbreak began in December 2019 in China and was rapidly expanded globally. Emergency measures, such as social distance or home confinement, were adopted by many country governments to prevent its transmission. In Spain, one of the most affected countries, the schools were closed, and one of the most severe mandatory home confinement was established for children from 14th March to 26th April 2020. The hypothesis of this study was that the measures adopted during the COVID-19 pandemic may have negatively affected physical activity and screen time of children. However, few studies have examined the effects of COVID-19 pandemic on lifestyle behaviours. Thus, the aim of the current work was to analyse the effects of the COVID-19 confinement on physical activity and screen time in Spanish children. For the current purpose, a total of 113 children and adolescents (12.0 ± 2.6 yr., 51.3% boys, 24.0% with overweight/obesity according to the World Obesity Federation) of the MUGI project were included in the analyses. Physical activity and screen time were longitudinally assessed by 'The Youth Activity Profile' questionnaire (YAP). Differences in physical activity and screen time before and during the confinement were assessed by dependent t-test. Before the confinement, 60% did not meet physical activity recommendations ( ≥ 60/min/day of moderate to vigorous physical activity), and 61% used screens ≥ 2 h/day. During the COVID-19 confinement, children decreased their physical activity levels (-91 ± 55 min/day, p < 0.001) and increased screen time ( ± 2.6 h/day, p < 0.001). The prevalence of children that worsened physical activity and screen time during the COVID-19 confinement were 95.2% and 69.8%, respectively. The current study evidence the negative effects of the COVID-19 confinement on physical activity and screen time in Spanish children. These findings should be taken into account to develop and implement future public health strategies for preserving children's lifestyle behaviours and health during and after the COVID-19 pandemic.

Keywords: COVID-19, lifestyle changes, paediatric, physical activity, screen time

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Authors: Raviv Harris, Maggie Levy

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Natural product-based pesticides may serve as an alternative to the traditional synthetic pesticides, which have a potentially damaging effect, both to human health and for the environment. Along with plants, microorganisms are a prospective source of such biological pesticides. A unique and active strain of P. aphidis (designated isolate L12, Israel 2004), an epiphytic and non-pathogenic basidiomycete yeast, was isolated in our lab from strawberry leaves. P. aphidis L12 secretions were found to inhibit broad range of plant pathogens. This work demonstrates that metabolites isolated from the biocontrol agent P. aphidis (isolate L12) can inhibit varied fungal and bacterial phytopathogens. Biologically active metabolites were extracted from P. aphidis biomass, using the organic solvent ethyl acetate. The antimicrobial activity of the extract was demonstrated, both in vitro and in planta. Using disk diffusion assays, the following inhibition zones were obtained: 43cm² for Pseudomonas syringae pv. tomato, 28.5cm² for Xanthomonas campestris pv. vesicatoria, 59cm² for Clavibacter michiganensis subsp. michiganensis, 34cm² for Erwinia amylovora and 34cm² for Agrobacterium tumefaciens. Additionally, strong inhibitory activity of the extract against fungi mycelial growth was established, with IC₅₀ values of 606µg ml⁻¹ for Botrytis cinerea, 221µg ml⁻¹ for Pythium spp., 519µg ml⁻¹ for Rhizoctonia solani, 455µg ml⁻¹ for Sclerotinia sclerotiorum, 2270µg ml⁻¹ for Fusarium oxysporum f. sp. lycopersici, and 2038µg ml⁻¹ for Alternaria alternata. The results of the in planta experiments demonstrated a dose-dependent reduction in disease infection. Significant inhibition of B. cinerea lesions on tomato plants was obtained when a spore suspension of this pathogen was treated with extract concentrations higher than 4.2mg ml⁻¹. Concentration of 7mg ml⁻¹ caused a reduction of over 95% in the lesion size of B. cinerea on tomato plants. The strong antimicrobial activity demonstrated both in vitro and in planta against varied phytopathogens, may indicate that the extracted antimicrobial metabolites have potential to serve as natural pesticides in the field.

Keywords: antimicrobial, B. cinerea, metabolites, natural pesticides, P. aphidis

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Authors: Harshada Vaidya-Kannur, Dattatraya Naik

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Propolis, one of the beehive products also referred as bee-glue is sticky dark coloured complex mixture of compounds. The volatile oil can be isolated from the propolis by hydrodistillation. The mark that is left behind after the removal of volatile oil is referred as the de-oiled propolis. Antioxidant as well as anti-inflammatory properties of total ethanolic extract of de-oiled propolis (TEEDP) was investigated. Another lot of deoiled propolis was successively exacted with hexane, ethyl acetate and ethanol. Activities of these fractions were also determined. Antioxidant activity was determined by studying ABTS, DPPH and NO radical scavenging. Determination of anti-inflammatory activity was carried out by topical TPA induced mouse ear oedema model. It is noteworthy that ethyl acetate fraction of deoiled propolis (EAFDP) exhibited 49.45 % TEAC activity at the concentration 0.2 mg/ml which is equivalent to the activity of trolox at the concentration 0.2 mg/ml. Its DPPH scavenging activity (72.56%) was closely comparable to that of trolox (75%). However its NO scavenging activity was comparatively low. From IC50 values it could be concluded that the efficiency of scavenging ABTS radicals by the de-oiled propolis was more pronounced as compared to scavenging of other radicals. Studies by TPA induced mouse ear inflammation model indicated that the de-oiled propolis of Indian origin had significant topical anti-inflammatory activity. The EAFDP was found to be the most active fraction for this activity also. The purification of EAFP yielded six pure crystalline compounds. These compounds were identified by their physical data and spectral data.

Keywords: anti-inflammatory activity, anti-oxidant activity, column chromatography, de-oiled propolis

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Authors: Maryam Kiani

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Non-precious electrocatalysts play a crucial role in the oxygen reduction reaction (ORR) for regenerative fuel cells and rechargeable metal-air batteries. To enhance ORR activity, La (a less active element) is added to modify the activity of Ni. This addition increases the surface contents of Ni2+, N, and S species in LaNi/N-S-C, while still maintaining a substantial specific surface area and hierarchical porosity. Therefore, the additional La is essential for the successful ORR process.In addition, the presence of extra La in the LaNi/N-S-C electrocatalyst enhances the efficiency of charge transfer and improves the surface acid-base characteristics, facilitating the adsorption of oxygen molecules during the ORR process. As a result, this superior and desirable electrocatalyst exhibits significantly enhanced ORR bifunctional activity. In fact, its ORR activity is comparable to that of the 20 wt% Pt/C.

Keywords: fuel cells, batteries, dual-doped carbon black, ORR

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Authors: Khadidja Bouzid, Fouzia Benali Toumi, Mohamed Bouzouina

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We made a comparison between the total phenolic content, concentrations of flavonoids and antioxidant activity of four different extracts (butanol, ethyl acetate, chloroform, water) of Arbutus unedo L. fruit (Ericacea) of El Marsa and Terni area. The total phenolic content in the extracts was determined using the Folin-Ciocalteu reagent and it ranged between 26.57 and 48.23 gallic acid equivalents mg/g of dry weight of extract. The concentrations of flavonoids in plant extracts varied from 17.98 to 56.84 catechin equivalents mg/g. The antioxidant activity was analyzed in vitro using the DPPH reagent; among all extracts, ethyl acetate fraction from El Marsa area showed the highest antioxidant activity.

Keywords: antioxidant activity, Arbutus unedo L., fruit flavonoids, phenols, Western Algeria

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Authors: T. O. Adejumo, O. S. Akinyemi

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Powders and oils of Aframomum melegueta, Garcinia kola and Piper guineense were tested as preservatives for the storage of maize grains for four weeks. The concentrations of the powders were 32.5gkg-1, 65.0gkg-1 and 97.5gkg-1 maize, while those of oils were 0.85mlkg-1, 0.50mlkg-1 and 0.75mlkg-1 maize respectively. Powders of the three botanicals at 97.5gkg-1 maize possessed insecticidal effect on Sitophilus zeamais and also inhibitory activities on Aspergillus flavus, A. fumigatus, A. niger and Fusarium verticillioides, while little effect was observed for other concentrations. Oils of the three botanicals at 0.50mlkg-1 and 0.75mlkg-1 maize showed an insecticidal effect on S. zeamais and also inhibitory activities on A. flavus, A. fumigatus, A. niger, F. verticillioides, Penicillium and Rhizopus species. Oils showed more potential as a protectant against fungal and insect pest in storage maize grains than powders. Powders and oils of A. melegueta, G. kola and P. guineense could be successfully used as biopesticides.

Keywords: aframomum melegueta, garcinia kola, maize, powder, oils, piper guineense

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Authors: Md. Aftabuzzaman, Md. Kamruzzaman

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Road-related expenditure and building construction activity are two significant drivers of the Victorian economy. This paper investigates the relationship between building construction activity and road-related expenditure. Data for construction activities were collected from Victorian Building Authority, and road-related expenditure data were explored by the Bureau of Infrastructure and Transport Research Economics. The trend between these two sectors was compared. The analysis found a strong relationship between road-related expenditure and the volume of construction activity, i.e., the more construction activities, the greater the requirement of road-related expenditure, or vice-versa. The road-related expenditure has a two-year lag period, suggesting that the road sector requires two years to respond to the growth in the building sector.

Keywords: building construction activity, infrastructure, road expenditure, Victorian Building Authority

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Authors: Zohreh Bayat, Dariush Minai-Tehrani

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Lipases constitute one of the most important groups of industrial enzymes that catalyze the hydrolysis of triacylglycerol to glycerol and fatty acids. Muscarinic antagonist relieves smooth muscle spasm of the gastrointestinal tract and effect on the cardiovascular system. In this research, the effect of a muscarinic antagonist on the lipase activity of Pseudomonas aeruginosa was studied. Lineweaver–Burk plot showed that the drug inhibited the enzyme by competitive inhibition. The IC50 value (60 uM) and Ki (30 uM) of the drug revealed the drug bound to the enzyme with high affinity. Determination of enzyme activity in various pH and temperature showed that the maximum activity of lipase was at pH 8 and 60°C both in presence and absence of the drug.

Keywords: bacteria, inhibition, kinetics, lipase

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Authors: Cheng-Yen Lu, Chin-Yuan Hsu

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Ambient temperature reduction (ATR) can extend the lifespan of an annual fish (Nothobranchius rachovii), but the underlying mechanism is unknown. In this study, the expression, concentration, and activity of cellular-degraded molecules were evaluated in the muscle of N. rachovii reared under high (30 °C), moderate (25 °C), and low (20 °C) ambient temperatures by biochemical techniques. The results showed that (i) the activity of the 20S proteasome, the expression of microtubule-associated protein 1 light chain 3-II (LC3-II), the expression of lysosome-associated membrane protein type 2a (Lamp 2a), and lysosome activity increased with ATR; (ii) the expression of the 70 kD heat shock cognate protein (Hsc 70) decreased with ATR; (iii) the expression of the 20S proteasome, the expression of lysosome-associated membrane protein type 1 (Lamp 1), the expression of molecular target of rapamycin (mTOR), the expression of phosphorylated mTOR (p-mTOR), and the p-mTOR/mTOR ratio did not change with ATR. These findings indicated that ATR activated the activity of proteasome, macroautophagy, and chaperone-mediated autophagy. Taken together these data reveal that ATR likely activates cellular degradation activity to extend the lifespan of N. rachovii.

Keywords: ambient temperature reduction, autophagy, degradation activity, lifespan, proteasome

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Authors: Liang Ning, Chung Hau Yin

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Angiogenesis is the process of new blood vessel development. It has been recognized as a therapeutic target for blocking cancer growth four decades ago. Vascular sprouting is initiated by pro-angiogenic factors. Vascular endothelial cell growth factor (VEGF) plays a central role in angiogenic initiation, many patients with cancer or ocular neovascularization have been benefited from anti-VEGF therapy. Emerging approaches impacting in the later stages of vessel remodeling and maturation are expected to improve clinical efficacy. TIE receptor as well as the corresponding angiopoietin ligands, were identified as another endothelial cell specific receptor tyrosine kinase signaling system. Much efforts were made to reduce the activity of angiopoietin-TIE receptor axis. Two eudesmane-type sesquiterpenes from laggera alata, namely, 15-dihydrocostic acid and ilicic acid were found with strong anti-angiogenic properties in zebrafish model. Meanwhile, the mRNA expression levels of VEGFR2 and TIE2 pathway related genes were down-regulated in the sesquiterpenes treated zebrafish embryos. Besides, in human umbilical vein endothelial cells (HUVECs), the sesquiterpenes have the ability to inhibit VEGF-induced HUVECs proliferation and migration at non-toxic concentration. Moreover, angiopoietin-2 induced TIE2 phosphorylation was inhibited by the sesquiterpenes, the inhibitory effect was detected in angiopoietin-1 induced HUVECs proliferation as well. Thus, we hypothesized the anti-angiogenic activity of the compounds may via the inhibition of VEGF and TIE2 related pathways. How the compounds come into play as the pathways inhibitors need to be evaluated in the future.

Keywords: Laggera alata, eudesmane-type sesquiterpene, anti-angiogenesis, VEGF, angiopoietin, TIE2

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Authors: Christophe Gonçalves, Raquel P. F. Guiné, Daniela Teixeira, Fernando J. Gonçalves

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Blueberries are widely valued for their high content in phenolic compounds with antioxidant activity, and hence beneficial for the human health. In this way, a study was done to determine the phenolic composition (total phenols, anthocyanins and tannins) and antioxidant activity of blueberries from three cultivars (Duke, Bluecrop, and Ozarblue) grown in two different Portuguese farms. Initially two successive extractions were done with methanol followed by two extractions with aqueous acetone solutions. These extracts obtained were then used to evaluate the amount of phenolic compounds and the antioxidant activity. The total phenols were observed to vary from 4.9 to 8.2 mg GAE/g fresh weight, with anthocyanin’s contents in the range 1.5-2.8 mg EMv3G/g and tannins contents in the range 1.5- 3.8 mg/g. The results for antioxidant activity ranged from 9.3 to 23.2 mol TE/g, and from 24.7 to 53.4 mol TE/g, when measured, respectively, by DPPH and ABTS methods. In conclusion it was observed that, in general, the cultivar had a visible effect on the phenols present, and furthermore, the geographical origin showed relevance either in the phenols contents or the antioxidant activity.

Keywords: anthocyanins, antioxidant activity, blueberry cultivar, geographical origin, phenolic compounds

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Authors: Naoki Ohshima, Ken Kaminishi

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Four types of dependencies, which are 'Finish-to-start', 'Finish-to-finish', 'Start-to-start' and 'Start-to-finish (S-F)' as logical relationship are modeled based on the definition by 'the predecessor activity is defined as an activity to come before a dependent activity in a schedule' in PMBOK. However, it is found a self-contradiction in the precedence diagram for S-F relationship by PMBOK. In this paper, author would like to validate logical relationship of S-F by Graph Theory and propose a new interpretation of the precedence diagram for S-F relationship.

Keywords: project time management, sequence activity, start-to-finish relationship, precedence diagram, PMBOK

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Authors: Uchenna Nkiruka Umeononihu, Adenike Kuku, Oludele Odekanyin, Olubunmi Babalola, Femi Agboola, Rapheal Okonji

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In this study, a lectin from the bulb of Dioscorea bulbifera was purified, characterised, and its acute and sub-acute toxicity was investigated with a view to evaluate its toxic effects in mice. The protein from the bulb was extracted by homogenising 50 g of the bulb in 500 ml of phosphate buffered saline (0.025 M) of pH 7.2, stirred for 3 hr, and centrifuged at the speed of 3000 rpm. Blood group and sugar specificity assays of the crude extract were determined. The lectin was purified in a two-step procedure- gel filtration on Sephadex G-75 and affinity chromatography on Sepharose 4-B arabinose. The degree of purity of the purified lectin was ascertained by SDS-polyacrylamide gel electrophoresis. Detection of covalently bound carbohydrate was carried out with Periodic Acid-Schiffs (PAS) reagent staining technique. Effects of temperature, pH, and EDTA on the lectin were carried out using standard methods. This was followed by acute toxicity studies via oral and subcutaneous routes using mice. The animals were monitored for mortality and signs of toxicity. The sub-acute toxicity studies were carried out using rats. Different concentrations of the lectin were administered twice daily for 5 days via the subcutaneous route. The animals were sacrificed on the sixth day; blood samples and liver tissues were collected. Biochemical assays (determination of total protein, direct bilirubin, Alanine aminotransferase (ALT), Aspartate aminotransferase (AST), catalase (CAT), and superoxide dismutase (SOD)) were carried out on the serum and liver homogenates. The collected organs (heart, liver, kidney, and spleen) were subjected to histopathological analysis. The results showed that lectin from the bulbs of Dioscorea bulbifera agglutinated non-specifically the erythrocytes of the human ABO system as well as rabbit erythrocytes. The haemagglutinating activity was strongly inhibited by arabinose and dulcitol with minimum inhibitory concentrations of 0.781 and 6.25, respectively. The lectin was purified to homogeneity with native and subunit molecular weights of 56,273 and 29,373 Daltons, respectively. The lectin was thermostable up to 30 0C and lost 25 %, 33.3 %, and 100 % of its heamagglutinating activity at 40°C, 50°C, and 60°C, respectively. The lectin was maximally active at pH 4 and 5 but lost its total activity at pH eight, while EDTA (10 mM) had no effect on its haemagglutinating activity. PAS reagent staining showed that the lectin was not a glycoprotein. The sub-acute studies on rats showed elevated levels of ALT, AST, serum bilirubin, total protein in serum and liver homogenates suggesting damage to liver and spleen. The study concluded that the aerial bulb of D. bulbifera lectin was non-specific in its heamagglutinating activity and dimeric in its structure. The lectin shared some physicochemical characteristics with lectins from other Dioscorecea species and was moderately toxic to the liver and spleen of treated animals.

Keywords: Dioscorea bulbifera, heamagglutinin, lectin, toxicity

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Authors: A. Kistaubayeva, I. Savitskaya, D. Ibrayeva, M. Abdulzhanova, N. Voronova

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36 strains of sulfur-oxidizing bacteria were isolated in Southern Kazakhstan soda-saline soils and identified. Screening of strains according bio-oxidation (destruction thiosulfate to sulfate) and enzymatic (Thiosulfate dehydrogenises and thiosulfate reductase) activity was conducted. There were selected modes of aeration and culture conditions (pH, temperature), which provide optimum harvest cells. These strains can be used in bio-melioration technology.

Keywords: elemental sulfur, oxidation activity, Тhiobacilli, fertilizers, heterotrophic S-oxidizers

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Authors: Monthon Tangjitmungman

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Numerous diseases have been linked to oxidative stress, in which a disproportion of free radicals in the body leads to tissue or cell damage. Polyphenols are the most abundant antioxidants found in plants, and they are highly effective at scavenging oxidative free radicals. Due to the presence of phenolic compounds in Caesalpinia sappan has been discovered to have antioxidant activity. It has several health benefits, the most important of which is preventing cardiovascular and cancer diseases. This study aimed to determine the phenolic content and antioxidant activity of C. sappan extract using a variety of antioxidant assays. The extract of C. sappan was made using a mixture of solvents (ethyl alcohol: water in ratio 8:2). The total phenolic content of C. sappan extract was determined and expressed as gallic acid equivalents using the Folin-Cioucalteu method (GAE). The antioxidant activity of C. sappan extract was assessed using the 2, 2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging assay and the ABTS radical scavenging capacity assay. An association was found between antioxidant activity and total phenol content. The antioxidant activity of C. sappan extract was also determined by DPPH and ABTS assays. The IC50 values for C. sappan extract from DPPH and ABTS assays were 54.48 μg/mL ± 0.545 and 25.46 μg/mL ± 0.790, respectively, in the DPPH assay. In the DPPH assay, vitamin C was used as a positive control, whereas Trolox was used as a positive control in the ABTS assay. In conclusion, C. sappan extract contains a high level of total phenolics and exhibits significant antioxidant activity. Nevertheless, more research should be done on the antioxidant activity, such as SOD and ROS scavenging assays and in vivo experiments, to determine whether the compound has antioxidant activity.

Keywords: ABTS assay, antioxidant activity, Caesalpinia sappan, DPPH assays, total phenolic content

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Authors: Kriyapa lairungruang, Arunporn Itharat

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Limonia acidissima L. (LA) (Common name: wood apple, Thai name: ma-khwit) is a medicinal plant which has long been used in Thai traditional medicine. Its bark is used for treatment of diarrhea, abscess, wound healing and inflammation and it is also used in oral cancer. Thus, this research aimed to investigate antioxidant and cytotoxic activities of the LA bark extracts produced by various extraction methods. Different extraction procedures were used to extract LA bark for biological activity testing: boiling in water, maceration with 95% ethanol, maceration with 50% ethanol and water boiling of each the 95% and the 50% ethanolic residues. All extracts were tested for antioxidant activity using DPPH radical scavenging assay, cytotoxic activity against human laryngeal epidermoid carcinoma (HEp-2) cells and human oral epidermoid carcinoma (KB) cells using sulforhodamine B (SRB) assay. The results found that the 95% ethanolic extract of LA bark showed the highest antioxidant activity with EC50 values of 29.76±1.88 µg/ml. For cytotoxic activity, the 50% ethanolic extract showed the best cytotoxic activity against HEp-2 and KB cells with IC50 values of 9.55±1.68 and 18.90±0.86 µg/ml, respectively. This study demonstrated that the 95% ethanolic extract of LA bark showed moderate antioxidant activity and the 50% ethanolic extract provided potent cytotoxic activity against HEp-2 and KB cells. These results confirm the traditional use of LA for the treatment of oral cancer and laryngeal cancer, and also support its ongoing use.

Keywords: antioxidant activity, cytotoxic activity, Laryngeal epidermoid carcinoma, Limonia acidissima L., oral epidermoid carcinoma

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