Search results for: alpha activity

Authors: Maryam Tajadod

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The treatment of cancer is one of the main challenges of nuclear medicine; while cancer begins in an organ, such as the breast or prostate, it spreads to the bone, resulting in metastatic bone. In the treatment of cancer with radiotherapy, the determination of the involved tissues’ dose is one of the important steps in the treatment protocol. Comparing absorbed doses for Lu-177 and Ra-223 and Ac-225 in the bone marrow and soft tissue of bone phantom with evaluating energetic emitted particles of these radionuclides is the important aim of this research. By the use of MCNPX computer code, a model for bone phantom was designed and the values of absorbed dose for Ra-223 and Ac-225, which are Alpha emitters & Lu-177, which is a beta emitter, were calculated. As a result of research, in comparing gamma radiation for three radionuclides, Lu-177 released the highest dose in the bone marrow and Ra-223 achieved the lowest level. On the other hand, the result showed that although the figures of absorbed dose for Ra and Ac in the bone marrow are near to each other, Ra spread more energy in cortical bone. Moreover, The alpha component of the Ra-223 and Ac-225 have very little effect on bone marrow and soft tissue than a beta component of the lu-177 and it leaves the highest absorbed dose in the bone where the source is located.

Keywords: bone metastases, lutetium-177, radium-223, actinium-225, absorbed dose

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Authors: Akrpoum Souad, Lalaoui Korrichi

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Vicia faba L.,Vaccinium macrocarpon, Punica granatum, Lavandula officinalis, Artemisia absinthium, Linum capitatum and Camellia sinensis were frequently used in our alimentation. In this study, we have tested the antimicrobial activity of their ethanolic and methanolic extracts on some pathogen bacteria, then their ability to in vivo inhibit the growth of Strepcoccus pneumonia. The phytochemical screening has given the composition of the most active extracts. According to the obtained results, the ethanolic extract of Lavendula. officinalis and A absinthium has shown an inhibition of all the tested strains of becteria3. The ethanolic extract of L. officinalis has given the highest activity against S. pneumoniae, followed by the methanolic extract of C. sinensis 1, 2 and P. granatum. The phytochemical screening showed that the most active extracts contained mainly naturels compounds.

Keywords: plants, extracts, antimicrobial activity, streptococcus pneumoniae, phytochemical screening

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Authors: Siti Helmyati, Euis Nurdiyawati, Joko Susilo, Endri Yuliati, Siti Fadhilatun Nashriyah, Kurnia Widyastuti

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Background: Iron fortification is one of the most effective and sustainable strategies to overcome anemia. It contradictively, has negative effect on gut microbiota balance. Pathogenic bacteria required iron for their growth. The iron source have greatly affect iron absorption in the intestine. Probiotic can inhibit the growth of pathogen. Lactobacillus plantarum Dad 13, Indonesian local isolate provides many benefits for health while fructo-oligosaccharides (FOS) provides selective substrates for probiotics’ growth. Objective: To determine the effect of iron fortification (NaFeEDTA and FeSO4) on antibacterial activity of synbiotic fermented milk. Methods: The antibacterial activity test was performed using the disc diffusion method. Paper discs were soaked in three kinds of synbiotic fermented milk, which are: 1) fortified with NaFeEDTA, 2) FeSO4 and 3) control. Escherichia coli was inoculated on nutrient agar medium. The ability of inhibition was shown by the formation of clear zone around the paper disc and measured in diameter (mm). Results: Synbiotic fermented milk fortified with iron (either NaFeEDTA or FeSO4) had antibacterial activity against Escherichia coli with diameter of clear zone were 6.53 mm and 12.3 mm, respectively (p<0.05). Compared to control (10.73 mm), synbiotic fermented milk fortified with FeSO4 had similar antibacterial activity (p>0.05). Conclusions: In vitro, synbiotic fermented milk fortified with NaFeEDTA and FeSO4 had different antibacterial activity against Escherichia coli. Iron fortification compound affected the antibacterial activity of synbiotic fermented milk.

Keywords: lactobacillus plantarum Dad 13, FOS, NaFeEDTA, FeSO4, antibacterial activity

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Authors: Mariane G. Tadros, Shahira M. Ezzat, Maha M. Salama, Mohamed A. Farag

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In this study, the in vitro anticholinesterase activity of the volatile oils of both O. basilicum and O. africanum was investigated and both samples showed significant activity. As a result, the major constituents of the two oils were isolated using several column chromatography. Linalool, 1,8-cineol and eugenol were isolated from the volatile oil of O. basilicum and camphor was isolated from the volatile oil of O. africanum. The anticholinesterase activity of the isolated compounds were also evaluated where 1,8-cineol showed the highest inhibitory activity followed by camphor. To confirm these activities, learning and memory enhancing effects were tested in mice. Memory impairment was induced by scopolamine, a cholinergic muscarinic receptor antagonist. Anti-amnesic effects of both volatile oils and their terpenoids were investigated by the passive avoidance task in mice. We also examined their effects on brain acetylcholinesterase activity. Results showed that scopolamine-induced cognitive dysfunction was significantly attenuated by administration of the volatile oils and their terpenoids, eugenol and camphor, in the passive avoidance task and inhibited brain acetylcholinesterase activity. These results suggest that O. basilicum and O. africanum volatile oils can be good candidates for further studies on Alzheimer’s disease via their acetylcholinesterase inhibitory actions.

Keywords: Ocimum baselicum, Ocimum africanum, GC/MS analysis, anticholinesterase

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Authors: Nadjib Melkemi, Salah Belaidi

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Quantitative Structure-Activity Relationship (QSAR) studies have been performed on nineteen molecules of 1,2-dithiole-3-thione analogues. The compounds used are the potent inducers of enzymes involved in the maintenance of reduced glutathione pools as well as phase-2 enzymes important to electrophile detoxication. A multiple linear regression (MLR) procedure was used to design the relationships between molecular descriptor and detoxication properties of the 1,2-dithiole-3-thione derivatives. The predictivity of the model was estimated by cross-validation with the leave-one-out method. Our results suggest a QSAR model based of the following descriptors: qS2, qC3, qC5, qS6, DM, Pol, log P, MV, SAG, HE and EHOMO for the specific activity of quinone reductase; qS1, qS2, qC3, qC4, qC5, qS6, DM, Pol, logP, MV, SAG, HE and EHOMO for the production of growth hormone. To confirm the predictive power of the models, an external set of molecules was used. High correlation between experimental and predicted activity values was observed, indicating the validation and the good quality of the derived QSAR models.

Keywords: QSAR, quinone reductase activity, production of growth hormone, MLR

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Authors: M. Ouassaf, S. Belaidi

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Aromatase is an estrogen biosynthetic enzyme belonging to the cytochrome P450 family, which catalyzes the limiting step in the conversion of androgens to estrogens. As it is relevant for the promotion of tumor cell growth. A set of thirty 1,2,3-triazole derivatives was used in the quantitative structure activity relationship (QSAR) study using regression multiple linear (MLR), We divided the data into two training and testing groups. The results showed a good predictive ability of the MLR model, the models were statistically robust internally (R² = 0.982) and the predictability of the model was tested by several parameters. including external criteria (R²pred = 0.851, CCC = 0.946). The knowledge gained in this study should provide relevant information that contributes to the origins of aromatase inhibitory activity and, therefore, facilitates our ongoing quest for aromatase inhibitors with robust properties.

Keywords: aromatase inhibitors, QSAR, MLR, 1, 2, 3-triazole

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Authors: Cheeze Janito, Crisly Dawang

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It is important to determine the personality traits that exist in the workplace and the contribution of these personality traits in the staff’s daily work routines; a sedentary lifestyle is harmful to one’s health. This study reports the personality traits of the University of Southern Mindanao, Kabacan, Philippines, non-teaching staff, the physical activity involvement of the non-teaching staff, and the big five personality traits that shape the relationship of university non-teaching staff in engaging physical activities. A quantitative method approach, which comprised a three-part questionnaire, was used to collect the data. The fifty non-teaching staff complete the survey. The results revealed that among the big five personality traits, the university non-teaching staff scored higher in agreeableness as revealed, that there was a commonality among the respondents’ traits of consideration to the feelings of the co-workers in observance to not being rude and vividly display of respect to co-workers and workplace and scored least in the personality trait of neuroticism. The study also reported that the university non-teaching staff's main physical activity was house chores as a prime physical exercise in which respondents reported a physical activity frequency of once to twice a week; thus, this study reported that the respondents are less engaged in doing physical activities. Further, the relationship of personality traits and the physical activity of the non-teaching staff gained a p-value of .596 that indicates there is no significant relationship between the two variables, the personality trait and physical activities. This study recommends the tight promotion of staff in engaging in physical activity of at least one hundred fifty minutes of moderate-intensity activity each week. Added to this, the use of different platforms containing physical exercise literacy and the benefits of physical exercise for the holistic development of the university community.

Keywords: university staff, physical fitness, personality traits, physical activity

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Authors: Farhad Azadi, Mohammad Mahdi Mohammadi, Mohsen Vahedi, Zahra Mahdiin

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Context: The aging population is growing all over the world and maintaining physical activity is essential for healthy aging. However, fear of falling is a major obstacle to physical activity among the elderly. The aim of this study is to investigate and compare the relationship between fear of falling and physical activity in Iranian urban and rural elderly. Research Aim: The main aim of this cross-sectional analytical study is to investigate and compare the relationship between fear of falling and physical activity in Iranian rural and urban elderly. Methodology: The study used simple non-probability sampling to select 350 participants aged 60 years and older from rural and urban areas of Konarak, Sistan and Baluchistan provinces in Iran. The Persian versions of the Falls Efficacy Scale - International, Rapid Physical Activity Assessment, Activities of Daily Living, and Instrumental Activities of Daily Living questionnaires were used to assess fear of falling and physical activity. The data were analyzed using Pearson correlation tests. Findings: The study found a statistically significant negative correlation between fear of falling and physical activity, as measured by ADL, IADL, and RAPA1(aerobic ), in all elderly and rural and urban elderly (p<0.001). Fear of falling was higher in rural areas, while physical activity levels measured by ADL and RAPA1 were higher in urban areas. No significant difference was found between the two groups in IADL and RAPA2 (strength and flexibility) scores. Theoretical Importance: This study highlights the importance of considering the fear of falling as a significant obstacle to proper physical activity, especially among the elderly living in rural areas. Furthermore, the study provides insight into the difference between rural and urban elderly people in terms of fear of falling and physical activity. Data Collection and Analysis Procedures: Data was collected through questionnaires and analyzed using Pearson correlation tests. Questions Addressed: The study attempted to answer the following questions: Is there a relationship between fear of falling and physical activity in Iranian urban and rural elderly people? Is there a difference in fear of falling and physical activity between rural and urban elderly? Conclusion: Fear of falling is a major obstacle to physical activity among the elderly, especially in rural areas. The study found a significant negative correlation between fear of falling and physical activity in all elderly and rural and urban elderly. In addition, urban and rural elderly have differences in aerobic activity levels, but they do not differ in terms of flexibility and strength. Therefore, proper interventions are required to ensure that the elderly can maintain physical activity, especially in rural and deprived areas.

Keywords: aged, fear of falling, physical activity, urban population, rural population

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Authors: Nassim Belkacem, Amina Azzam, Dalila Haouchine, Kahina Bennacer, Samira Soufit

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Objective: To evaluate the antioxidant activity of the methanolic extract along with the antimicrobial activity of the essential oil of the aerial parts of Rosmarinus officinalis L. collected in the region of Bejaia (northern center of Algeria). Materials and methods: The polyphenols and flavonoids contents of the methanolic extract were measured. The antioxidant activity was evaluated using two methods: the ABTS method and DPPH assay. The antimicrobial activity was studied by the agar diffusion method against five bacterial strains (Three Gram positive strains and two Gram negative strains) and one fungus. Results: The total polyphenol and flavonoid content was about 43.8 mg gallic acid equivalent per gram (GA Eq/g) and 7.04 mg quercetin equivalent per gram (Q Eq/g), respectively. In the ABTS assay, the rosemary extract has shown an inhibition of 98.02% at the concentration of 500ug/ml with a half maximal inhibitory concentration value (IC50) of 194.92ug/ml. The results of DPPH assay have shown that the rosemary extract has an inhibition of 94.67 % with an IC50 value of 17.87ug/ml, which is lower than that of Butylhydroxyanisol (BHA) about 6.03ug/ml and ascorbic acid about 1.24μg/ml. The yield in essential oil of rosemary obtained by hydrodistillation was 1.42%. Based on the determination of the diameter of inhibition, different antimicrobial activity of the essential oil was revealed against the six tested microbes. Escherichia coli from the University Hospital (UH), Streptococcus aureus (UH) and Pseudomonas aeruginosa ATCC have a minimum inhibitory concentration value (MIC) of 62.5µl/ml. However, Bacillus sp (UH) and Staphylococcus aureus ATCC have an MIC value of 125μl/ml. The inhibition zone against Candida sp was about 24 mm. The aromatograms showed that the essential oil of rosemary exercises an antifungal activity more important than the antibacterial one.

Keywords: Rosmarinus officinalis L., maceration, essential oil, antioxidant, antimicrobial activity

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Authors: Linda Chularojmontri, Seewaboon Sireeratawong, Suvara Wattanapitayakul

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Terminalia arjuna Roxb. (family Combretaceae) is commonly known as ‘Sa maw thet’ in Thai. The fruit is used in traditional medicine as natural mild laxatives, carminative and expectorant. Aim of the study: This research aims to study the anti-inflammatory, analgesic and antipyretic activities of Terminalia arjuna extract by using animal models in comparison to the reference drugs. Materials and Methods: The anti-inflammatory study was conducted by two experimental animal models namely ethyl phenylpropionate (EPP)-induced ear edema and carrageenan-induced paw edema. The study of analgesic activity used two methods of pain induction including acetic acid and heat-induced pain. In addition, the antipyretic activity study was performed by induced hyperthermia with yeast. Results: The results showed that the oral administration of Terminalia arjuna extract possessed acute anti-inflammatory effect in carrageenan-induced paw edema. Terminalia arjuna extract showed the analgesic activity in acetic acid-induced writhing response and heat-induced pain. This indicates its peripheral effect by inhibiting the biosynthesis and/or release of some pain mediators and some mechanism through Central nervous system. Moreover, Terminalia arjuna extract at the dose of 1000 and 1500 mg/kg body weight showed the antipyretic activity, which might be because of the inhibition of prostaglandins. Conclusion: The findings of this study indicated that the Terminalia arjuna extract possesses the anti-inflammatory, analgesic and antipyretic activities in animals.

Keywords: analgesic activity, anti-inflammatory activity, antipyretic activity, Terminalia arjuna extract

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Authors: Dipanshu Sur, Ratnabali Chakravorty, Rimi Pal, Siddhartha Chatterjee, Joyshree Chaterjee, Amal Mallik

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Background: Women with polycystic ovary disease (PCOD) frequently suffer from metabolic disturbances. PCOD is a common ovulatory disorder in young women, which affects 5-10% of the population and results in infertility due to anovulation. Importantly, aromatase in ovarian granulosa and luteinized granulosa cells plays an important role for women of reproductive age. Generation and metabolism of androgen is directly related to aromatase activity. The E2/T ratio provides important information about aromatase activity because conversion of androgens to estrogens is mediated by CYP19, suggesting that the E2/T ratio may be a direct marker of aromatase activity. The nature of the interaction between ovarian aromatase activity and PCOD in women has been controversial, and the impact of weight gain on aromatase activity as well as E2 levels is unknown. Aim: The objective of this study was to investigate the association and relation between aromatase activity and levels of body mass index (BMI) from a reproductive hormone perspective in a group of women with or without PCOD. Methods: We designed a cohort study which included 200 individuals. It enrolled 100 cases of PCOD based on 2006 Rotterdam criteria and 100 ovulatory normal- non PCOD, healthy, age-matched controls. Plasma sex hormones viz. estradiol (E2), testosterone (T), follicle stimulating hormone (FSH), and luteinizing hormone (LH) were measured by ELISA on the second day of the menstrual cycle, together with BMI and E2/T were calculated. Aromatase activity in PCOD patients with different BMI, T and E2 levels were compared. Results: PCOD patients showed significantly increased levels of BMI, E2 (P=0.004), T and LH, while their E2/T (P= <0.001), FSH and FSH/LH values were decreased compared with the control group. Higher E2 levels correlated with a relatively enhanced E2/T as well as T and LH levels but reduced BMI, FSH and FSH/LH levels in women with PCOD. Hyperandrogenic PCOD patients had increased E2 levels but their aromatase activity was markedly inhibited independent of their BMI values. Conclusions: We found a significant decrease of ovarian aromatase activity in women with PCOD as compared to controls. Our study showed that ovarian aromatase activity in PCOD was decreased which was independent of BMI. Enhancing aromatase activity may become an optimized strategy for developing therapies for PCOD women, especially those with obesity.

Keywords: aromatase activity, polycystic ovary disease, obesity, body mass index

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Authors: Hulya Tuba Kiyan, Nilgun Ozturk

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Gentiana, a member of Gentianaceae, is represented by approximately 400 species in the world and 12 species in Turkey. Flavonoids, iridoids, triterpenoids and also xanthones are the major compounds of this genus, have been previously reported to have antiinflammatory, antimicrobial, antioxidant, hepatoprotective, hypotensive, hypoglycaemic, DNA repair and immunomodulatory properties. The methanolic extract of the aerial parts of Gentiana brachyphylla Vill. from Turkey was evaluated for its biological activities and its total phenolic content in the present study. According to the antioxidant activity results, G. brachyphylla methanolic extract showed very strong anti-DNA damage antioxidant activity with an inhibition of 81.82%. It showed weak ferric-reducing power with a EC50 value of 0.65 when compared to BHT (EC50 = 0.2). Also, at 0.5 mg/ml concentration, the methanolic extract inhibited ABTS radical cation activity with an inhibition of 20.13% when compared to Trolox (79.01%). Chelating ability of G. brachyphylla was 44.71% whereas EDTA showed 78.87% chelating activity at 0.2 mg/ml. Also G. brachyphylla showed weak 27.21% AChE, 20.23% BChE, strong 67.86% MAO-A and moderate 50.06% MAO-B, weak 19.14% COX-1, 29.11% COX-2 inhibitory activities at 0.25 mg/ml. The total phenolic content of G. brachyphylla was 156.23 ± 2.73 mg gallic acid equivalent/100 g extract.

Keywords: antioxidant activity, cholinesterase inhibitory activity, Gentiana brachyphylla Vill., total phenolic content

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Authors: L. L. Tundisi, A. Pessoa Jr., E. B. Tambourgi, E. Silveira, P. G. Mazzola

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L-asparaginase (L-ASNase) is the gold standard treatment for acute lymphoblastic leukemia that mainly affects pediatric patients; treatment increases survival from 20% to 90%. The characterization of other L-Asparaginases, apart from the most used from Escherichia coli and Erwinia chrysanthemi, has been reported, but the choice of the most appropriate is still under debate. This choice should be based on its pharmacokinetics, immune hypersensitivity, doses, prices, pharmacodynamics. The main factors influencing the antileukemic activity of ASNase are enzymatic activity, Km, glutaminase activity, clearance of the enzyme and development of resistance. However, most of the commercialized enzyme present an intrinsic glutaminase activity, which is responsible for some side effects. In this study, glutaminase free asparaginase produced from Aspergillus oryzae was precipitated in different percentages of ethanol (0–80%), until optimum ethanol concentration of 60% (w/w) was found. Following, precipitation of crude L-ASNase was performed in a single step, using 60% (w/w) ethanol, under constant agitation and temperature. It presented activity of 135.45 U/mg and after gel filtration chromatography with Sephadex G-the enzymatic activity was 322.02 U/mg. The apparent molecular mass of the purified L-ASNase fraction was estimated by 10% SDS-PAGE. Proteins were stained with Coomassie Brilliant Blue R-250. The molar mass range was from 10 kDa to 250 kDa. L-ASNase from Aspergillus oryzae was characterized aiming possible therapeutic use. Four different buffers (phosphate-citrate buffer pH 2.6 to 5.8; phosphate buffer pH 5.8 to 7.4; Tris - HCl pH 7.4 to 9.0; and carbonate buffer pH 9.8 to 10.6) were used to measure the optimum pH for L-ASNase activity. The optimum temperature for enzyme activity was measured at optimal pH conditions (Tris-HCl and phosphate buffer, pH 7.4) at different temperatures ranging from 5 to 55°C. All activities were calculated by quantifying the free ammonia, using the Nessler reagent. The kinetic parameters calculation, e.g. Michaelis-Menten constant (Km), maximum velocity (Vmax) and Hills coefficient (n), were performed by incubating the enzyme in different concentrations of the substrate at optimum conditions of pH and fitted on Hill’s equation. This glutaminase free asparaginase showed a low Km (3.39 mM and 3.81 mM) and enzymatic activity of 135.45 U/mg after precipitation with ethanol. After gel filtration chromatography it rose to 322.02 U/mg. Optimum activity was found between pH 5.8 - 9.0, best activity results with phosphate buffer pH 7.4 and Tris-HCl pH 7.4 and showed activity from 5°C to 55°C. These results indicate that L-ASNase from A. oryzae has the potential for human use.

Keywords: biopharmaceuticals, bioprocessing, bioproducts, biotechnology, enzyme activity, ethanol precipitation

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Authors: Irina Deputat, Anatoly Gribanov, Yuliya Dzhos, Alexandra Nekhoroshkova, Tatyana Yemelianova, Irina Bolshevidtseva, Irina Deryabina, Yana Kereush, Larisa Startseva, Tatyana Bagretsova, Irina Ikonnikova

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In the modern world the number of elderly people increases. Preservation of functionality of an organism in the elderly becomes very important now. During aging the higher cortical functions such as feelings, perception, attention, memory, and ideation are gradual decrease. It is expressed in the rate of information processing reduction, volume of random access memory loss, ability to training and storing of new information decrease. Perspective directions in studying of aging neurophysiological parameters are brain imaging: computer electroencephalography, neuroenergy mapping of a brain, and also methods of studying of a neurodynamic brain processes. Research aim – to study features of a brain aging in elderly people by electroencephalogram (EEG) and the DC-potential level. We examined 130 people aged 55 - 74 years that did not have psychiatric disorders and chronic states in a decompensation stage. EEG was recorded with a 128-channel GES-300 system (USA). EEG recordings are collected while the participant sits at rest with their eyes closed for 3 minutes. For a quantitative assessment of EEG we used the spectral analysis. The range was analyzed on delta (0,5–3,5 Hz), a theta - (3,5–7,0 Hz), an alpha 1-(7,0–11,0 Hz) an alpha 2-(11–13,0 Hz), beta1-(13–16,5 Hz) and beta2-(16,5–20 Hz) ranges. In each frequency range spectral power was estimated. The 12-channel hardware-software diagnostic ‘Neuroenergometr-KM’ complex was applied for registration, processing and the analysis of a brain constant potentials level. The DC-potential level registered in monopolar leads. It is revealed that the EEG of elderly people differ in higher rates of spectral power in the range delta (р < 0,01) and a theta - (р < 0,05) rhythms, especially in frontal areas in aging. By results of the comparative analysis it is noted that elderly people 60-64 aged differ in higher values of spectral power alfa-2 range in the left frontal and central areas (р < 0,05) and also higher values beta-1 range in frontal and parieto-occipital areas (р < 0,05). Study of a brain constant potential level distribution revealed increase of total energy consumption on the main areas of a brain. In frontal leads we registered the lowest values of constant potential level. Perhaps it indicates decrease in an energy metabolism in this area and difficulties of executive functions. The comparative analysis of a potential difference on the main assignments testifies to unevenness of a lateralization of a brain functions at elderly people. The results of a potential difference between right and left hemispheres testify to prevalence of the left hemisphere activity. Thus, higher rates of functional activity of a cerebral cortex are peculiar to people of early advanced age (60-64 years) that points to higher reserve opportunities of central nervous system. By 70 years there are age changes of a cerebral power exchange and level of electrogenesis of a brain which reflect deterioration of a condition of homeostatic mechanisms of self-control and the program of processing of the perceptual data current flow.

Keywords: brain, DC-potential level, EEG, elderly people

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Authors: Ibrahim M. Labouta, Marwa H. El-Wakil, Hayam M. Ashour, Ahmed M. Hassan, Manal N. Saudi

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The receptor tyrosine kinase c-Met is an attractive target for therapeutic treatment of cancers nowadays. Among the wide variety of heterocycles that have been explored for developing c-Met kinase inhibitors, the 1,2,4-triazines have been rarely investigated, although they are well known in the literature to possess antitumor activities. Herein we describe the design and synthesis of a novel series of 1,2,4-triazine derivatives possessing N-acylarylhydrazone moiety and another series combining the 1,2,4-triazine scaffold to the well-known anticancer drug 6-MP in order to explore their “double-drug” effect. The synthesized compounds were evaluated for their in vitro antitumor activity against three c-Met addicted cancer cell lines (A549, HT-29 and MKN-45). Most compounds showed moderate to excellent antiproliferative activity and four compounds showed potent inhibitory activity more than the reference drug Foretinib against one or more cancer cell lines. The obtained results revealed that the potent compounds are highly selective to A549 (lung adenocarcinoma) cancer cell line. The c-Met kinase inhibitory activity of the potent derivatives is still under investigation. The present study clearly demonstrates that the 1,2,4-triazine core ring exhibits promising antitumor activity with potential c-Met kinase inhibitory activity.

Keywords: 1, 2, 4-triazine, antitumor, c-Met inhibitor, double-drug

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Authors: Martyn Queen, Diane Crone, Andrew Parker, Saul Bloxham

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Rationale: There is a growing body of evidence that supports the use of physical activity during and after cancer treatment. However, activity levels for patients remain low. As more cancer patients are treated successfully, and treatment costs continue to escalate, physical activity may be a promising adjunct to a person-centred healthcare approach to recovery. Aim: The aim was to further understand how physical activity may enhance the recovery process for a group of mixed-site cancer patients. Objectives: The research investigated longitudinal changes in physical activity and perceived the quality of life between two and six month’s post-exercise interventions. It also investigated support systems that enabled patients to sustain these perceived changes. Method: The respondent cohort comprised 14 mixed-site cancer patients aged 43-70 (11 women, 3 men), who participated in a two-phase physical activity intervention that took place at a university in the South West of England. Phase 1 consisted of an eight-week structured physical activity programme; Phase 2 consisted of four months of non-supervised physical activity. Semi-structured interviews took place three times over six months with each participant. Grounded theory informed the data collection and analysis which, in turn, facilitated theoretical development. Findings: Our findings propose three theories on the impact of physical activity for recovering cancer patients: 1) Knowledge gained through a structured exercise programme can enable recovering cancer patients to independently sustain physical activity to four-month follow-up. 2) Sustaining physical activity for six months promotes positive changes in the quality of life indicators of chronic fatigue, self-efficacy, the ability to self-manage and energy levels. 3) Peer support from patients facilitates adherence to a structured exercise programme and support from a spouse, or life partner facilitates independently sustained physical activity to four-month follow-up. Conclusions: This study demonstrates that qualitative research can provide an evidence base that could be used to support future care plans for cancer patients. Findings also demonstrate that a physical activity intervention can be effective at helping cancer patients recover from the side effects of their treatment, and recommends that physical activity should become an adjunct therapy alongside traditional cancer treatments.

Keywords: physical activity, health, cancer recovery, quality of life, support systems, qualitative, grounded theory, person-centred healthcare

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Authors: Rajesh A. Rane, Shital S. Naphade, Rajshekhar Karpoormath

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Thiozolidin-4-one, a mimic of thiazolobenzimidazole (TBZ) has drawn many attentions due to its potent and selective inhibition against the HIV-1 and low toxicity by binding to the allosteric site of the reverse transcriptase (RT) as a non-nucleoside RT inhibitor (NNRTI). Similarly, marine bromopyrrole alkaloids are well known for their diverse array of anti-infective properties. Hence, we have reported synthesis and in vitro HIV-1 RT inhibitory activity of a series of 4-thiazolidinone-bromopyrrole alkaloid hybrids tethered with amide linker. The results of in vitro HIV-1 RT kit assay showed that some of the compounds, such as 4c, 4d, and 4i could effectively inhibit RT activity. Among them, compounds 4c having 4-chlorophenyl substituted 4-thiazolidione ring was the best one with the IC50 value of 0.26 µM. The sturdy emerges with key structure-activity relationship that pyrrole-NH-free core benefited inhibition against HIV-1 RT inhibition. This study identified conjugate 4c with potent activity and selectivity as promising compound for further drug development to HIV.

Keywords: antiviral drugs, bromopyrrole alkaloids, HIV-1 RT inhibition, 4-thiazolidinone

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Authors: Aline Giardin

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Introduction: This review addresses the relationship between physical education and mental health and its main objective is to discuss the meanings that circulate in Psychiatric Hospitalization Units and Psychosocial Care Centers (CAPS) about the presence of physical education teachers and the practices developed by Them within these services. Material and methods: It is based on the theoretical contribution of the Psychiatric Reform and is methodologically inspired by the Bibliographic Review. Objectives: The objective of this review was to identify the main scientific evidence on the effects of physical activity on the main psychological aspects associated with mental health during the hospitalization process. Results: It was observed that physical activity has beneficial effects in the psychological, social and cognitive aspects, being thus a fundamental aspect of the lifestyle in promoting a healthy and successful treatment. In studies evaluating the effects of physical activity on mental health, the most frequently evaluated outcomes include anxiety, depression, and health-related quality of life (eg, self-esteem and self-efficacy). Evidence from epistemological studies indicates that the level of physical activity is positively associated with good mental health, when mental health is defined as good mood, general well-being and decreased symptoms. Conclusion: It is necessary to intervene and a greater interest of the professionals of physical education in the treatment with the people with mental disorders so that the negative symptoms are modified, through the aid of the physical activity, by better quality of life, physical condition, nutritional state and A healthy emotional appearance.

Keywords: health mental, physical activity, benefits, treatment

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Authors: Robert Dutkiewicz, Monika Szpringer, Mariola Wojciechowska

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Physical activity is one of the factors greatly influencing healthy lifestyle. The recent research into physical activity of the Polish society reveals that contribution of physical culture to healthy lifestyle is insufficient. Students, regardless of age, spend most of free-time in front of a TV or computer. The research attempted to identify the level of physical activity and healthy lifestyle among students of medical sciences and other students doing their teaching degrees. The findings of physical activity research conducted in 2014, which covered 364 students of medical sciences and future teachers from the University of Jan Kochanowski in Kielce were analysed. The research involved the method of diagnostic survey based on a questionnaire. It attempted to establish to what extent such factors as the field of studies, the place of residence and BMI affect students’ physical activity. Empirical material was analysed by means of SPSS/PC, the leading statistical software. The field of study significantly influences physical activity of the respondents. The students of physiotherapy and public health tend to be more physically active than students of biology and geography: 46.8% students of geography and 51.8 % biology students seldom take up physical activity. Obesity and overweight are currently serious problems of university students: 6.6% of them are obese and 19% overweight. It is alarming that these students are not willing to find ways to be more physically active. Most of the obese and overweight respondents study biology or geography and live in a rural area. Unequal chances in terms of youth physical culture are determined by the differences between rural and urban environments. Young people living in rural areas are less physically active, particularly in terms of the frequency and the amount of time devoted to physical activity. This is caused by poor infrastructure to perform physical activity, the lack of or limited number of sports clubs and centres. It is thought-provoking that most of the students claim that they do not have enough time to do sports or other activities, but at the same time they spend a lot of time at a computer or watching TV.

Keywords: BMI, healthy lifestyle, sports activity, students

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Authors: Kheira A. Bekhechi, Belkacem Khiat

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The goal of our study is to know if there is an influence of the regular sporting physical-activity on the school performances of Algerian children. An experimental group composed of 55 sporting pupils and a reference group of 55 non-sporting pupils between 6 to10 years old (boys and girls) of the primary schools in Oran (Algeria) were followed during 15 months (Five terms). The socio-demographic data was collected from a survey given to pupils of the two groups and the school results from the administration at the end of each term. The sporting pupils have a general school average significantly higher than those of the non- sporting pupils (p < 0.05). The practice of physical activity and regular sporting by the children would deserve to be largely encouraged based on the beneficial effects not only on health but also on the academic performance. The parents, teachers and health professionals should be strongly aware.

Keywords: cognitive capacities, physical activity and sport, school children, school performances

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Authors: Mannan Malik Muhammad Naeem, Jeong Myung Yung

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Functional near infrared spectroscopy (fNIRS) has a favorable position in non-invasive brain imaging techniques. The concentration change of oxygenated hemoglobin and de-oxygenated hemoglobin during particular cognitive activity is the basis for this neuro-imaging modality. Two wavelengths of near-infrared light can be used with modified Beer-Lambert law to explain the indirect status of neuronal activity inside brain. The temporal resolution of fNIRS is very good for real-time brain computer-interface applications. The portability, low cost and an acceptable temporal resolution of fNIRS put it on a better position in neuro-imaging modalities. In this study, an optimization model for impulse response function has been used to estimate/predict initial dip using fNIRS data. In addition, the activity strength parameter related to motor based cognitive task has been analyzed. We found an initial dip that remains around 200-300 millisecond and better localize neural activity.

Keywords: fNIRS, brain-computer interface, optimization algorithm, adaptive signal processing

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Authors: Dina Helmy El-Ghonemy, Thanaa Hamed Ali

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The aim of this study was to purify and characterize a keratinolytic enzyme produced by Aspergillus sp. DHE7 cultured in basal medium containing chicken feather as substrate. The enzyme was purified through ammonium sulfate saturation of 60%, followed by gel filtration chromatography in Sephadex G-100, with a 16.4-purification fold and recovery yield of 52.2%. Sodium dodecyl sulfate-polyacrylamide gel electrophoresis revealed that the purified enzyme is a monomeric enzyme with an apparent molecular mass of 30 kDa — the purified keratinase of Aspergillus sp. DHE7 exhibited activity in a broad range of pH (7- 9) and temperature (40℃-60℃) profiles with an optimal activity at pH eight and 50℃. The keratinolytic activity was inhibited by protease inhibitors such as phenylmethylsulfonyl fluoride and ethylenediaminetetraacetate, while no reduction of activity was detected by the addition of dimethyl sulfoxide (DMSO). Bivalent cations, Ca²⁺ and Mn²⁺, were able to greatly enhance the activity of keratinase by 125.7% and 194.8%, respectively, when used at one mM final concentration. On the other hand, Cu²⁺ and Hg²⁺ inhibited the enzyme activity, which might be indicative of essential vicinal sulfhydryl groups of the enzyme for productive catalysis. Furthermore, the purified keratinase showed significant stability and compatibility against the tested commercial detergents at 37ºC. Therefore, these results suggested that the purified keratinase from Aspergillus sp. DHE7 may have potential use in the detergent industry and should be of interest in the processing of poultry feather waste.

Keywords: Aspergillus sp. DHE7, biochemical characterization, keratinase, purification, waste management

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Authors: K. Biswas, U. H. Armin, S. M. J. Prodhan, J. A. Prithul, S. Sarker, F. Afrin

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Alzheimer’s disease (AD) (a progressive neurodegenerative disorder) is mostly predominant cause of dementia in the elderly. Prolonging the function of acetylcholine by inhibiting both acetylcholinesterase and butyrylcholinesterase is most effective treatment therapy of AD. Traditionally Pterocarpus santalinus L. is widely known for its medicinal use. In this study, in vitro acetylcholinesterase inhibitory activity was investigated and methanolic extract of the plant showed significant activity. To confirm this activity (in vivo), learning and memory enhancing effects were tested in mice. For the test, memory impairment was induced by scopolamine (cholinergic muscarinic receptor antagonist). Anti-amnesic effect of the extract was investigated by the passive avoidance task in mice. The study also includes brain acetylcholinesterase activity. Results proved that scopolamine induced cognitive dysfunction was significantly decreased by administration of the extract solution, in the passive avoidance task and inhibited brain acetylcholinesterase activity. These results suggest that bark extract of Pterocarpus santalinus can be better option for further studies on AD via their acetylcholinesterase inhibitory actions.

Keywords: Pterocarpus santalinus, cholinesterase inhibitor, passive avoidance, Alzheimer’s disease

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Authors: Chin-Yuan Hsu, Yu-Lung Chuang

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The expression, concentration, and activity of mitochondrial energy-utilized molecules and cellular energy-regulated molecules decreased with age in the trophocytes and oenocytes of honeybees (Apis mellifera), but those of cellular energy-metabolized molecules is unknown. In this study, the expression, concentration, and activity of cellular energy-metabolized molecules were assayed in the trophocytes and fat cells of young and old worker bees by using the techniques of cell and biochemistry. The results showed that (i) the •-hydroxylacyl-coenzyme A dehydrogenase (HOAD) activity/citrate synthase (CS) activity ratio, non-esterified fatty acids concentrations, the expression of eukaryotic initiation factor 4E, and the expression of phosphorylated eIF4E binding protein 1 decreased with age; (ii) fat and glycogen accumulation increased with age; and (iii) the pyruvate dehydrogenase (PDH) activity/citrate synthase (CS) activity ratio was not correlated with age. These finding indicated that •-oxidation (HOAD/CS) and protein synthsis decreased with age. Glycolysis (PDH/CS) was unchanged with age. The most likely reason is that sugars are the vital food of worker bees. Taken together these data reveal that young workers have higher cellular energy metabolism than old workers and that aging results in a decline in the cellular energy metabolism in worker honeybees.

Keywords: aging, energy, honeybee, metabolism

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Authors: S. Raeis Farshid, B. Raeis Farshid

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Ag-TiO₂ nanocomposites were prepared by the sol-gel method with and without additives such as carboxy methyl cellulose (CMC), polyethylene glycol (PEG), polyvinyl pyrrolidone (PVP), and hydroxyl propyl cellulose (HPC). The characteristics of the prepared Ag-TiO₂ nanocomposites were identified by Fourier Transform Infra-Red spectroscopy (FTIR), X-Ray Diffraction (XRD), and scanning electron microscopy (SEM) methods. The additives have a significant effect on the particle size distribution and photocatalytic activity of Ag-TiO₂ nanocomposites. SEM images have shown that the particle size distribution of Ag-TiO₂ nanocomposite in the presence of HPC was the best in comparison to the other samples. The photocatalytic activity of the synthesized nanocomposites was investigated for decolorization of methyl orange (MO) in water under UV-irradiation in a batch reactor, and the results showed that the photocatalytic activity of the nanocomposites had been increased by CMC, PEG, PVP, and HPC, respectively.

Keywords: sol-gel method, Ag-TiO₂, decolorization, photocatalyst, nanocomposite

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Authors: Khalida Boutemak, Nasssima Benali, Nadji Moulai-Mostefa

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Effect of enzyme on the yield and chemical composition of Artemisia campestris essential oil is reported in the present study. It was demonstrated that enzyme facilitated the extraction of essential oil with increase in oil yield and did not affect any noticeable change in flavour profile of the volatile oil. Essential oil was tested for antibacterial activity using Escherichia coli; which was extremely sensitive against control with the largest inhibition (29mm), whereas Staphylococcus aureus was the most sensitive against essential oil obtained from enzymatic pre-treatment with the largest inhibition zone (25mm). The antioxidant activity of the essential oil with hemicellulase pre-treatment (EO2) and control sample (EO1) was determined through reducing power. It was significantly lower than the standard drug (vitamin C) in this order: vitamin C˃EO2˃EO1.

Keywords: Artemisia campestris, enzyme pre-treatment, hemicellulase, antibacterial activity, antioxidant activity

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Authors: Ana Tsokilauri

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The uppermost factor in the regulation of lignin-cellulose activity of decaying white rot or free rot are the substances serving as carbon and nitrogen nutrition of microorganisms and are considered as the most important factor of generative activity of white rot. The research object was Basidiomycete Fungi, peculiar and common in Georgia, and the separation of 10 of them as pure crops. The unidentified pure crops have tasted in order to be determined the potential of synthesis of lignin-degrading enzymes and the substrate of optimal lignocellulose growth. One of the most important aspects of the research conducted on Basidiomycetes was the use of specific lignocellulosic residues for selecting Fungi as a substrate of their growth. In order to increase lignocellulose with the help of substrate, crops were selected from the screening stage that showed good laccase activity. (Dusheti 1; Dusheti 10; Fshavi 5; Fshavi1; Fshavi 8; Fshavi 32; Manglisi 26; Sabaduri20; Dusheti 7; Sabaduri 1 ), Among the selected cultures, the crops with good laccase activity against the following substances, in particular: Dusheti 1- in this case, the rate of enzymatic activity on bran substrate was -105,6 u/ml, mandarin-96,4 u/ml. In case of corn - 102,9 u/ml. In case of Dusheti 7- the indicators were as follows: bananas-121,7 u/ml, mandarin-125,4 u/ml, corn - 117,1 u/ml. In the case of Sanaduri 32, the laccase activity was as follows: pomegranate- 101,2 u/ml. As a result of conducted experiments, the synthesis and activity rates of enzymes depending on plant substrates varied within a fairly wide range, which is still being under research.

Keywords: Lignocellulosic substrate, Basidiomycetes, white-rot basidiomycetes, Laccase

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Authors: Omaimah Algohary

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Kaolin is one of the principle intestinal adsorbents, has traditionally been used internally in the treatment of various enteric disorders, colitis, enteritis, dysentery, and diarrhea associated with food and alkaloidal poisoning and in traveler’s diarrhea. It binds to and traps bacteria and its toxins and gases in the gut. It also binds to water in the gut, which helps to make the stools firmer, hence giving symptomatic relief. Metronidazole is a synthetic antibacterial agent that is used primarily in the treatment of various anaerobic infections such as intra-abdominal infections, antiprotozoal, and as amebicidal. The need for safe, therapeutically effective antidiarrheal combination continuously lead to effective treatment. Metronidazol used for treatment of anaerobic bacteria and kaolin , when administered simultaneously, Metronidazole–Kaolin interactions have been reported by FDA but not studied. This project is the first to study the effect of Metronidazole–Kaolin interactions on the antimicrobial activity of metronidazole. Agar diffusion method performed to test the antimicrobial activity of metronidazole–kaolin antidiarrheal combination from aqueous solutions at an in-vivo simulated pHs conditions that obtained at 37+0.5 °C on Helicobacter pylori as anaerobic bacteria and E.coli as aerobic bacteria and used as a control for the technique. The antimicrobial activity of metronidazole combination as 1:1 and 1:2 with kaolin was abolished in acidic media as no zones of inhibition shown compared to only metronidazole that used as a control. In alkaline media metronidazole combination as 1:1 and 1:2 with kaolin showed diminutive activity compared to the control. These results proved that the kaolin adsorb metronidazole and abolish its antimicrobial activity and such combination should be avoided.

Keywords: kaolin, metronidazole, interaction, Helicobacter pylori. E. coli, antimicrobial activity

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Authors: Aruma Baduge Kithma Hansanee De Silva

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Haskap (Lonicera caerulea L.), also known as blue honeysuckle, is a recently commercialized berry crop in Canada. Haskap berries are rich in polyphenols, including anthocyanins, which are known for potential health-promoting effects. Cyanidin-3-O-glucoside (C3G) is the most prominent anthocyanin of haskap berries. Recent literature reveals the efficacy of C3G in reducing the risk of type 2 diabetes (T2D), which has become an increasingly common health issue around the world. The T2D is characterized as a metabolic disorder of hyperglycemia and insulin resistance. It has been demonstrated that C3G has anti-diabetic effects in various ways, including improvement in insulin sensitivity, and inhibition of activities of carbohydrate-hydrolyzing enzymes, including alpha-amylase and alpha-glucosidase. The goal of this study was to investigate the influence of variety and harvesting date on haskap composition, biological properties, and antidiabetic properties. The polyphenolic compounds present in four commercially grown haskap cultivars, Aurora, Rebecca, Larissa and Evie among five harvesting stages (H1-H5), were extracted separately in 80% ethanol and analyzed to characterize their phenolic profiles. The haskap berries contain different types of polyphenols including flavonoids and phenolic acids. Anthocyanin is the major type of flavonoid. C3G is the most prominent type of anthocyanin, which accounts for 79% of total anthocyanin in all extracts. The variety Larissa at H5 contained the highest average C3G content, and its ethanol extract had the highest (1212.3±63.9 mg/100g FW) while, Evie at H1 contained the lowest C3G content (96.9±40.4 mg/100g FW). The average C3G content of Larissa from H1 – H5 varies from 208 – 1212 mg/100g FW. Quarcetin-3-Rutinoside (Q3Rut) is the major type of flavonol and highest is observed in Rebecca at H4 (47.81 mg/100g FW). The haskap berries also contained phenolic acids, but approximately 95% of the phenolic acids consisted of chlorogenic acid. The cultivar Larissa has a higher level of anthocyanin than the other four cultivars. The highest total phenolic content is observed in Evie at H5 (2.97±1.03 mg/g DW) while the lowest in Rebecca at H1 (1.47±0.96 mg/g DW). The antioxidant capacity of Evie at H5 was higher (14.40±2.21 µmol TE/ g DW) among other cultivars and the lowest observed in Aurora at H3 (5.69±0.34 µmol TE/ g DW). Furthermore, Larissa H5 shows the greatest inhibition of carbohydrate-hydrolyzing enzymes including alpha-glucosidase and alpha-amylase. In conclusion Larissa, at H5 demonstrated highest polyphenol composition and antidiabetic properties.

Keywords: anthocyanin, cyanidin-3-O-glucoside, haskap, type 2 diabetes

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Authors: Heidarali Malmir

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The effects of acid rain (AR), smog’s cars (SC), and combined AR+SC on the antioxidants enzymes, lipid-soluble antioxidants, and water-soluble antioxidants were studied in the two cultivars of rice. The results showed that simulated AR significantly increased the total glutathione (TGSH), thiobarbituric acid (TBA), and α-tocopherol, accompanied by decreases in dry weight and leaves area in the two cultivars, and this change was more obvious in Shirudi cultivar than in Aus cultivar (p≤0.05). Under SC stress cultivar shirudi had higher H+-ATPase, glutathione peroxidase (GSH-px), and catalase (CAT) activities than cultivar Aus. The results of superoxide dismutase (SOD) activity, TGSH, and α-tocopherol levels affected by AR treatments were very different to those of SOD activity, TGSH, and α-tocopherol levels, as shown in SC treatment. It seems that SOD activity coupled with the water-soluble antioxidants and α-tocopherol levels correlated with the lipid-soluble antioxidants. It is suggested that α-tocopherol increases H+-ATPase activity.

Keywords: H+-ATPase, membrane permeability, lipid soluble antioxidants, water soluble antioxidants, associated enzyme

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