Search results for: xanthine oxidase inhibitory activity

Authors: Vaibhav Budhiraja, Chandra Mouli Pandey

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The ultrasonic synthesis of nanostructured conducting copolymer is an effective technique to synthesize polymer with desired chemical properties. This tailored nanostructure, shows tremendous improvement in sensitivity and stability to detect a variety of analytes. The present work reports ultrasonically synthesized nanostructured conducting poly(o-phenylenediamine)-co-poly(1-naphthylamine) (POPD-co-PNA). The synthesized material has been characterized using Fourier transform infrared spectroscopy (FTIR), ultraviolet-visible spectroscopy, transmission electron microscopy, X-ray diffraction and cyclic voltammetry. FTIR spectroscopy confirmed random copolymerization, while UV-visible studies reveal the variation in polaronic states upon copolymerization. High crystallinity was achieved via ultrasonic synthesis which was confirmed by X-ray diffraction, and the controlled morphology of the nanostructures was confirmed by transmission electron microscopy analysis. Cyclic voltammetry shows that POPD-co-PNA has rather high electrochemical activity. This behavior was explained on the basis of variable orientations adopted by the conducting polymer chains. The synthesized material was electrophoretically deposited at onto indium tin oxide coated glass substrate which is used as cathode and parallel platinum plate as the counter electrode. The fabricated bioelectrode was further used for detection of glucose by crosslinking of glucose oxidase in the PODP-co-PNA film. The bioelectrode shows a surface-controlled electrode reaction with the electron transfer coefficient (α) of 0.72, charge transfer rate constant (ks) of 21.77 s⁻¹ and diffusion coefficient 7.354 × 10⁻¹⁵ cm²s⁻¹.

Keywords: conducting, electrophoretic, glucose, poly (o-phenylenediamine), poly (1-naphthylamine), ultrasonic

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Authors: N. Tadayon, H. Yousefnia, S. Zolghadri, A. Ramazani, A. R. Jalilian

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In this study, 68Ga-PDTMP was prepared as a new agent for bone imaging. 68Ga was obtained from SnO2 based generator. A certain volume of the PDTMP solution was added to the vial containing 68GaCl3 and the pH of the mixture was adjusted to 4 using HEPES. Radiochemical purity of the radiolabelled complex was checked by thin layer chromatography. Biodistribution of this new agent was assessed in rats after intravenously injection of the complex. For this purpose, the rats were killed at specified times after injection and the weight and activity of each organ was measured. Injected dose per gram was calculated by dividing the activity of each organ to the total injected activity and the mass of each organ. As expected the most of the activity was accumulated in the bone tissue. The radiolabelled compound was extracted from blood very fast. This new bone-seeking complex can be considered as a good candidate of PET-based radiopharmaceutical for imaging of bone metastases.

Keywords: biodistribution, Ga-68, imaging, PDTMP

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Authors: Chanasit Chaocharoenphat

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Hibiscus sabdariffa is a herbal plant that is commonly used for home remedies in Thailand. This study aims to determine the antioxidant activity of polyphenols, as oxidative stress plays a vital role in the development of cancer, and H. sabdariffa was used in this study. The total flavonoids content was determined using the aluminium chloride colourimetric method and expressed as quercetin equivalents (QE)/g and the antioxidant capacity of the flavonoids using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical scavenging capacity assays. The IC50 values of H. sabdariffa extract were 167.14 μg/mL ± 0.843 and 77.59 μg/mL ± 0.798, respectively. In the DPPH assay, vitamin C was used as a positive control, whereas Trolox was used as a positive control in the ABTS assay. To summarise, H. sabdariffa extract contains a high concentration of total flavonoids and exhibits potent antioxidant activity. However, additional antioxidant activity assays such as superoxide dismutase (SOD), reactive oxygen species (ROS), and reactive nitrogen species (RNS) scavenging assays and in vitro antioxidant experiments should be carried out to investigate the molecular mechanism of the compound.

Keywords: ABTS assay, antioxidant activity, Gracilaria fisheri, DPPH assays, total flavonoid content

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Authors: Kristina Karapetyan, Flora Tkhruni, Tsovinar Balabekyan, Arevik Israyelyan, Tatyana Khachatryan

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The ability of the lactic acid bacteria (LAB) to prevent and cure a variety of diseases, their protective role against infections and colonization of pathogenic microorganisms in the digestive tract, has lead to the coining of the term probiotics or pro-life. LAB inhibiting the growth of pathogenic and food spoilage microorganisms, maintaining the nutritive quality and improving the shelf life of foods. They have also been used as flavor and texture producers. Enterococcus strains have been used for treatment of diseases such as diarrhea or antibiotic associated diarrhea, inflammatory pathologies that affect colon such as irritable bowel syndrome, or immune regulation, diarrhea caused by antibiotic treatments. The obtaining and investigation of biological properties of proteinoceous antibiotics, on the basis of probiotic LAB shown, that bacteriocins, metabiotics, and peptides of LAB represent bactericides have a broad range of activity and are excellent candidates for development of new prophylactic and therapeutic substances to complement or replace conventional antibiotics. The genotyping by 16S rRNA sequencing for LAB were used. Cell free culture broth (CFC) broth was purified by the Gel filtration method on the Sephadex Superfine G 25 resin. Antimicrobial activity was determined by spot-on-lawn method and expressed in arbitrary units (AU/ml). The diversity of multidrug-resistance (MDR) of pathogenic strains to antibiotics, most widely used for treatment of human diseases in the Republics of Armenia and Nagorno Karabakh were examined. It was shown, that difference of resistance of pathogens to antibiotics depends on their isolation sources. The influences of partially purified antimicrobial preparations (AMP), obtained from the different strains of Enterococcus genus on the growth of MDR pathogenic bacteria were investigated. It was shown, that bacteriocin containing partially purified preparations, obtained from different strains of Enterococcus faecium and durans species, possess bactericidal or bacteriostatic activity against antibiotic resistant intestinal, spoilage and food-borne pathogens such as Listeria monocytogenes, Staphylococcus aureus, E. coli, and Salmonella. Endemic strains of LAB, isolated from Matsoni made from donkey, buffalo and goat milk, shown broad spectrum of activity against food spoiling microorganisms, moulds and fungi, such as Salmonella sp., Esherichia coli, Aspergillus and Penicillium species. Highest activity against MDR pathogens shown bacteria, isolated from goat milk products. High stability of the investigated strains of the genus Enerococcus, isolated from samples of matsun from different regions of Nagorno-Karabakh (NKR) to the antibiotics was shown. The obtained data show high stability of the investigated different strains of the genus Enerococcus. The high genetic diversity in Enterococcus group suggests adaptations for specific mutations in different environments. Thus, endemic strains of LAB are able to produce bacteriocins with high and different inhibitory activity against broad spectrum of microorganisms isolated from different sources and belong to different taxonomic group. Prospect of the use of certain antimicrobial preparations against pathogenic strains is obvious. These AMP can be applied for long term use against different etiology antibiotic resistant pathogens for prevention or treatment of infectional diseases as an alternative to antibiotics.

Keywords: antimicrobial biopreparation, endemic lactic acid bacteria, intra-species diversity, multidrug resistance of pathogens

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Authors: Stoyanka Georgieva Vladeva, Elena Kirilova Kirilova, Nikola Kirilov Kirilov

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Summary: WHO (World Health Organization) recommends the elder people a certain amount of regular physical activity in order to prevent some of the health issues. Postmenopausal osteoporosis is one of the chronic diseases which requires the maintaining of regular physical activity. The regular activity combined with an adequate medical treatment greatly improves the quality of life of the patient. Objectives: Assessment of the effect of the regular physical activity recommended by WHO on the quality of life in patients with postmenopausal osteoporosis. Material and methods: For the period of one year 68 female patients treated with Denosumab have been monitored. The bone density has been measured with the DEXA method in accordance to the T-score. No patients having any oncologic diseases and secondary osteoporosis have been included in the study. The subjects have been divided into groups by their age. The first group – women aged under 65 years (27 subjects) and the second group – women aged over 65 years (41 subjects). All patients have been advised to maintain regular physical activity included in the recommendations of the WHO in accordance with the age and the disease. The quality of life has been assessed in the beginning and at the end of the one-year period using the SF 36V2 questionnaire. Results: Only 31% of the subjects have engaged into regular increased physical activities for the whole period. Among them are mostly patients of the second group (aged over 65 years, 71%). The women from the both groups who were engaging into regular activities for this one-year period all experience an improvement of the quality of life. These results show that older patients understand the necessity of the physical activity for their health. The comparison of the output data to the scales of physical activity, durability, body pain, vitality, social activity and emotional stability has found an improvement at the end of the period in all patients. The osteodensitometry showed general improvement of the T-score. Patients with additional visits to their rheumatologist have better results. Conclusion: Combination of regular physical activity in accordance to the recommendations of WHO and medical treatment including anti-osteoporotic drugs improves the quality of life of women with postmenopausal osteoporosis.

Keywords: elderly patients, osteoporosis, physical activity, quality of life

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Authors: Jun Gil Ahn, Jong Kang Park, Jong Tae Kim

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In this paper, we analyze major components of activity recognition (AR) in wearable device with 9-axis sensors and sensor fusion filters. 9-axis sensors commonly include 3-axis accelerometer, 3-axis gyroscope and 3-axis magnetometer. We chose sensor fusion filters as Kalman filter and Direction Cosine Matrix (DCM) filter. We also construct sensor fusion data from each activity sensor data and perform classification by accuracy of AR using Naïve Bayes and SVM. According to the classification results, we observed that the DCM filter and the specific combination of the sensing axes are more effective for AR in wearable devices while classifying walking, running, ascending and descending.

Keywords: accelerometer, activity recognition, directiona cosine matrix filter, gyroscope, Kalman filter, magnetometer

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Authors: Warachate Khobjai, Suriyan Sukati, Khemjira Jarmkom, Pattaranut Eakwaropas, Surachai Techaoei

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The propose of this study was to investigate in vitro thrombolytic activity of Zingiber cassumunar Roxb. and Prasaplai, a Thai herbal formulation of Z. cassumunar Roxb. Herbs were extracted with boiling water and concentrated by lyophilization. To observe their thrombolytic potential, an in vitro clot lysis method was applied where streptokinase and sterile distilled water were used as positive and negative controls, respectively. Crude aqueous extracts from Z. cassumunar Roxb. and Prasaplai formula showed significant thrombolytic activity by clot lysis of 17.90% and 25.21%, respectively, compared to the negative control water (5.16%) while the standard streptokinase revealed 64.78% clot lysis. These findings suggest that Z. cassumunar Roxb. exhibits moderate thrombolytic activity and cloud play an important role in the thrombolytic properties of Prasaplai formula. However, further study should be done to observe in vivo clot dissolving potential and to isolate active component(s) of these extracts.

Keywords: thrombolytic activity, clot lysis, Zingiber cassumunar Roxb., Prasaplai formula, aqueous extract

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Authors: R. A. Abdel Rahman, A. E. Abdel Wahab, E. A. Goghneimy, H. F. Mohamed, E. M. Salama

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Infectious diseases are a major cause of death worldwide. The treatment of infections continues to be problematic in modern time because of the severe side effects of some drugs and the growing resistance to antimicrobial agents. Hence, the search for newer, safer and more potent antimicrobials is a pressing need. Herbal medicines have received much attention as a source of new antibacterial drugs since they are considered time-tested and comparatively safe both for human use and the environment. In the present study, the antimicrobial activity of marjoram (Origanum majorana L.) essential oil on some gram positive and gram negative reference bacteria, as well as some hospital resistant microbes, was tested. Marjoram oil was extracted and the oil chemical constituents were identified using GC/MS analysis. Staphylococcus aureas ATCC 6923, Pseudomonus auregonosa ATCC 9027, Bacillus subtilis ATCC 6633, E. coli ATCC 8736 and two hospital resistant microbes isolates 16 and 21 were used. The two isolates were identified by biochemical tests and 16s rRNA as proteus spp. and Enterococcus facielus. The effect of different concentrations of essential oils on bacterial growth was tested using agar disk diffusion assay method to determine the minimum inhibitory concentrations and using micro dilution method to determine the minimum bactericidal concentrations. Marjoram oil was found to be effective against both reference and hospital resistance strains. Hospital strains were more resistant to marjoram oil than reference strains. P. auregonosa growth was completely inhibited at a low concentration of oil (4µl/ml). The other reference strains showed sensitivity to marjoram oil at concentrations ranged from 5 to 7µl/ml. The two hospital strains showed sensitivity at media containing 10 and 15µl/ml oil. The major components of oil were terpineol, cis-beta (23.5%), 1,6 – octadien –3-ol,3,7-dimethyl, 2 aminobenzoate (10.9%), alpha terpieol (8.6%) and linalool (6.3%). Scanning electron microscope (SEM) and transmission electron microscope (TEM) analysis were used to determine the difference between treated and untreated hospital strains. SEM results showed that treated cells were smaller in size than control cells. TEM data showed that cell lysis has occurred to treated cells. Treated cells have ruptured cell wall and appeared empty of cytoplasm compared to control cells which shown to be intact with normal volume of cytoplasm. The results indicated that marjoram oil has a positive antimicrobial effect on hospital resistance microbes. Natural crude extracts can be perfect resources for new antimicrobial drugs.

Keywords: antimicrobial activity, essential oil, hospital resistance microbes, marjoram

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Authors: Nélio Veiga, Paula Ferreira, Tiago Correia, Maria J. Correia, Carlos Pereira, Odete Amaral, Ilídio J. Correia

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Introduction: The application of fissure sealants is considered to be an important primary prevention method used in dental medicine. However, the formation of microleakage gaps between tooth enamel and the fissure sealant applied is one of the most common reasons of dental caries development in teeth with fissure sealants. The association between various dental biomaterials may limit the major disadvantages and limitations of biomaterials functioning in a complementary manner. The present study consists in the incorporation of a cariostatic agent – silver diamine fluoride (SDF) – in a resin-based fissure sealant followed by the study of release kinetics by spectrophotometry analysis of the association between both biomaterials and assessment of the inhibitory effect on the growth of the reference bacterial strain Streptococcus mutans (S. mutans) in an in vitro study. Materials and Methods: An experimental in vitro study was designed consisting in the entrapment of SDF (Cariestop^® 12% and 30%) into a commercially available fissure sealant (Fissurit^®), by photopolymerization and photocrosslinking. The same sealant, without SDF was used as a negative control. The effect of the sealants on the growth of S. mutans was determined by the presence of bacterial inhibitory halos in the cultures at the end of the incubation period. In order to confirm the absence of bacteria in the surface of the materials, Scanning Electron Microscopy (SEM) characterization was performed. Also, to analyze the release profile of SDF along time, spectrophotometry technique was applied. Results: The obtained results indicate that the association of SDF to a resin-based fissure sealant may be able to increase the inhibition of S. mutans growth. However, no SDF release was noticed during the in vitro release studies and no statistical significant difference was verified when comparing the inhibitory halo sizes obtained for test and control group.  Conclusions: In this study, the entrapment of SDF in the resin-based fissure sealant did not potentiate the antibacterial effect of the fissure sealant or avoid the immediate development of dental caries. The development of more laboratorial research and, afterwards, long-term clinical data are necessary in order to verify if this association between these biomaterials is effective and can be considered for being used in oral health management. Also, other methodologies for associating cariostatic agents and sealant should be addressed.

Keywords: biomaterial, fissure sealant, primary prevention, silver diamine fluoride

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Authors: S.Kauroo, J. Govinden Soulange, D. Marie

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Psiadia species from the Asteraceae are traditionally used in the folk medicine of Mauritius to treat cutaneous and bronchial infections. The present study aimed at validating the phytomedicinal properties of the selected species from the Asteraceae family, namely Psiadia arguta, Psiadia viscosa, Psiadia lithospermifolia, and Distephanus populifolius. Dried hexane, ethyl acetate, and methanol leaf extracts were studied for their antioxidant properties using the DPPH (1, 1-diphenyl-2-picryl-hydrazyl), FRAP (Ferric Reducing Ability of Plasma), and Deoxyribose assays. Antibacterial activity against human pathogenic bacteria namely Escherichia coli (ATCC 27853), Staphylococcus aureus (ATCC 29213), Enterococcus faecalis (ATCC 29212), Klebsiella pneumonia (ATCC27853), Pseudomonas aeruginosa (ATCC 27853), and Bacillus cereus (ATCC 11778) was measured using the broth microdilution assay. Qualitative phytochemical screening using standard methods revealed the presence of coumarins, tannins, leucoanthocyanins, and steroids in all the tested extracts. The measured phenolics level of the selected plant extracts varied from 24.0 to 231.6 mg GAE/g with the maximum level in methanol extracts in all four species. The highest flavonoids and proanthocyanidins content was noted in Psiadia arguta methanolic extracts with 65.7±1.8 mg QE/g and 5.1±0.0 mg CAT/g dry weight (DW) extract, respectively. The maximum free radical scavenging activity was measured in Psiadia arguta methanol and ethyl acetate extracts with IC50 11.3±0.2 and 11.6± 0.2 µg/mL, respectively and followed by Distephanus populifolius methanol extracts with an IC50 of 11.3± 0.8 µg/mL. The maximum ferric reducing antioxidant potential was noted in Psiadia lithospermifolia methanol extracts with a FRAP value of 18.8 ± 0.4 µmol Fe2+/L/g DW. The antioxidant capacity based on DPPH and Deoxyribose values were negatively related to total phenolics, flavonoid and proanthocyanidins content while the ferric reducing antioxidant potential were strongly correlated to total phenolics, flavonoid and proanthocyanidins content. All four species exhibited antimicrobial activity against the tested bacteria (both Gram-negative and Gram-positive). Interestingly, the hexane and ethyl acetate extracts of Psiadia viscosa and Psiadia lithospermifolia were more active than the control antibiotic Chloramphenicol. The Minimum inhibitory concentration (MIC) values for hexane and ethyl acetate extracts of Psiadia viscosa and Psiadia lithospermifolia against the tested bacteria ranged from (62.5 to 500 µg/ml). These findings validate the use of these tested Asteraceae in the traditional medicine of Mauritius and also highlight their pharmaceutical potential as prospective phytomedicines.

Keywords: antibacterial, antioxidant, DPPH, flavonoids, FRAP, Psiadia spp

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Authors: Rossy G. Olan Villegas, Gerardo Acosta Garcia, Aurea Bernardino Nicanor, Leopoldo Gonzalez Cruz, Humberto Ramirez Medina

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Capsicum annuum is a crop of agricultural and economic importance in Mexico and other countries. The fruit (pepper) contains bioactive components such as carotenoids, phenolic compounds and capsaicinoids that improve health. However, pepper cultivation is affected by biotic and abiotic factors that decrease yield. Some phytohormones like gibberellins and auxins induce the formation and development of fruit in several plants. In this study, we evaluated the effect of the exogenous application of phytohormones like gibberellic acid and indolbutyric acid on fruit development of jalapeno pepper plants, the protein profile of plant tissues, the accumulation of bioactive compounds and antioxidant activity in the pericarp and seeds. For that, plants were sprinkled with these phytohormones. The fruit collection for the control, indolbutyric acid and gibberellic acid treatments was 7 peppers per plant; however, for the treatment that combines indolbutyric acid and gibberellic acid, a fruit with the shortest length (1.52 ± 1.00 cm) and weight (0.41 ± 1.0 g) was collected compared to fruits of plants grown under other treatments. The length (4,179 ± 0,130 cm) and weight of the fruit (8,949 ± 0.583 g) increased in plants treated with indolbutyric acid, but these characteristics decreased with the application of GA3 (length of 3,349 ± 0.127 cm and a weight 4,429 ± 0.144 g). The content of carotenes and phenolic compounds increased in plants treated with GA3 (1,733 ± 0.092 and 1,449 ± 0.009 mg / g, respectively) or indolbutyric acid (1,164 ± 0.042 and 0.970 ± 0.003 mg / g). However, this effect was not observed in plants treated with both phytohormones (0.238 ± 0.021 and 0.218 ± 0.004 mg / g). Capsaicin content was higher in all treatments; but it was more noticeable in plants treated with both phytohormones, the value being 0.913 ± 0.001 mg / g (three times greater in amount). The antioxidant activity was measured by 3 different assays, 2,2-diphenyl-1-picrylhydrazyl (DPPH), antioxidant power of ferric reduction (FRAP) and 2,2'-Azinobis-3-ethyl-benzothiazoline-6-sulfonic acid ( ABTS) to find the minimum inhibitory concentration of the reducing radical (IC50 and EC50). Significant differences were observed from the application of the phytohormone, being the fruits treated with gibberellins, which had a greater accumulation of bioactive compounds. Our results suggest that the application of phytohormones modifies the development of fruit and its content of bioactive compounds.

Keywords: auxins, capsaicinoids, carotenoids, gibberellins

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Authors: Sedef Şahin, Meral Huri

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Cerebral Palsy (CP) represents the most frequent cause of physical disability in children with a rate of 2,9 per 1000 live births. The activity-focused intervention is known to improve function and reduce activity limitations and barriers to participation of children with disabilities. The aim of the study was to assess the effects of occupational therapy on level of fatigue, activity performance and satisfaction in children with Unilateral Cerebral Palsy. Twenty-two children with hemiparetic cerebral palsy (mean age: 9,3 ± 2.1years; Gross Motor Function Classification System ( GMFCS) level from I to V (I = 54%, II = 23%, III = 14%, IV= 9%, V= 0%), Manual Ability Classification System (MACS) level from I to V (I = 40%, II = 32%, III = 14%, IV= 10%, V= 4%), were assigned to occupational therapy program for 6 weeks.Visual Analogue Scale (VAS) was used for intensity of the fatigue they experienced at the time on a 10 point Likert scale (1-10).Activity performance and satisfaction were measured with Canadian Occupational Performance Measure (COPM).A client-centered occupational therapy intervention was designed according to results of COPM. The results were compared with nonparametric Wilcoxon test before and after the intervention. Thirteen of the children were right-handed, whereas nine of the children were left handed.Six weeks of intervention showed statistically significant differences in level of fatigue, compared to first assessment(p<0,05). The mean score of first and the second activity performance scores were 4.51 ± 1.70 and 7.35 ± 2.51 respectively. Statistically significant difference between performance scores were found (p<0.01). The mean scores of first and second activity satisfaction scores were of 2.30± 1.05 and 5.51 ± 2.26 respectively. Statistically significant difference between satisfaction assessments were found (p<0.01). Occupational therapy is an evidence-based approach and occupational therapy interventions implemented by therapists were clinically effective on severity of fatigue, activity performance and satisfaction if implemented individually during 6 weeks.

Keywords: activity performance, cerebral palsy, fatigue, occupational therapy

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Authors: I. L. Ibrahim, A. Mann, A. Ndanaimi

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The research involved phytochemical screening, antibacterial activities and mineral determination by flame photometry of the crude extract of Brysocarpus coccineus schum indeed were carried out. The result of Phytochemical screening reveal tha saponins, alkaloids, cardiac glycosides, and anthraquinones were present. This suggests that the plant extract could be used as anti-inflammatory and anti-bleeding agents. Estimation of mineral content shows that the crude extract of B. coccineus contains 0.73 (Na+), 1.06 (K+) and 1.98 (Ca+) which justifies its use to be safe for hypertensive patients and could be used to lower blood pressure. The antibacterial properties of aqueous and ethanol extract were studied against some bacteria; pseudomonas aeruginosa, Escherichia coli, Bacilus subtilis, Klebsilla penmuoniae by disc diffusion method. The aqueous extract showed significant activity against the organisms while the ethanol at concentrations 5-10mg/ml ethanol extract showed significant zone of inhibition against the organisms, E. coli, (19 mm), B. cereus (12 mm), P. aeruginosa (11 mm), K. pnemuoniae (11 mm). Minimum inhibitory concentration (MIC) was carried with considerable effect of inhibition on the organisms. The MIC values observed were 1, 24, 16 and 19 mm against E. coli, B. cereus, P. aeruginosa and K. pnemuoniae respectively. Therefore, the plant could be a potential source of antibacterial agent although more pharmacological and clinical study may be recommended.

Keywords: phytochemicals, microorganisms, screenings, mineral ions

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Authors: Asma Ben Hmidene, Mizuho Hanaki, Kazuma Murakami, Kazuhiro Irie, Hiroko Isoda, Hideyuki Shigemori

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Type 2 diabetes mellitus (T2DM) and Alzheimer’s disease (AD) are characterized as a peripheral metabolic disorder and a degenerative disease of the central nervous system, respectively. It is now widely recognized that T2DM and AD share many pathophysiological features including glucose metabolism, increased oxidative stress and amyloid aggregation. Amyloid beta (Aβ) is the components of the amyloid deposits in the AD brain and while the component of the amyloidogenic peptide deposit in the pancreatic islets of Langerhans is identified as human islet amyloid polypeptide (hIAPP). These two proteins are originated from the amyloid precursor protein and have a high sequence similarity. Although the amino acid sequences of amyloidogenic proteins are diverse, they all adopt a similar structure in aggregates called cross-beta-spine. Add at that, extensive studies in the past years have found that like Aβ1-42, IAPP forms early intermediate assemblies as spherical oligomers, implicating that these oligomers possess a common folding pattern or conformation. These similarities can be used in the search for effective pharmacotherapy for DM, since potent therapeutic agents such as antioxidants with a catechol moiety, proved to inhibit Aβ aggregation, may play a key role in the inhibit the aggregation of hIAPP treatment of patients with DM. Tamarix gallica is one of the halophyte species having a powerful antioxidant system. Although it was traditionally used for the treatment of various liver metabolic disorders, there is no report about the use of this plant for the treatment or prevention of T2DM and AD. Therefore, the aim of this work is to investigate their protective effect towards T2DM and AD by isolation and identification of α-glucosidase inhibitors, with antioxidant potential, that play an important role in the glucose metabolism in diabetic patient, as well as, the polymerization of hIAPP and Aβ aggregation inhibitors. Structure-activity relationship study was conducted for both assays. And as for α-glucosidase inhibitors, their mechanism of action and their synergistic potential when applied with a very low concentration of acarbose were also suggesting that they can be used not only as α-glucosidase inhibitors but also be combined with established α-glucosidase inhibitors to reduce their adverse effect. The antioxidant potential of the purified substances was evaluated by DPPH and SOD assays. Th-T assay using 42-mer amyloid β-protein (Aβ42) for AD and hIAPP which is a 37-residue peptide secreted by the pancreatic β –cells for T2DM and Transmission electronic microscopy (TEM) were conducted to evaluate the amyloid aggragation of the actives substances. For α-glucosidase, p-NPG and glucose oxidase assays were performed for determining the inhibition potential and structure-activity relationship study. The Enzyme kinetic protocol was used to study the mechanism of action. From this research, it was concluded that polyphenols playing a role in the glucose metabolism and oxidative stress can also inhibit the amyloid aggregation, and that substances with a catechol and glucuronide moieties inhibiting amyloid-β aggregation, might be used to inhibit the aggregation of hIAPP.

Keywords: α-glucosidase inhibitors, amyloid aggregation inhibition, mechanism of action, polyphenols, structure activity relationship, synergistic potential, tamarix gallica

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Authors: Azhar Jabareen, Mahmoud Huleihel

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BRCA-1 is a multifunctional tumor suppressor, whose expression is activated by the estrogen (E2)-liganded ERα receptor. The activated ERα is a transcriptional factor which activates various genes either by direct binding to the DNA at E2-responsive elements (EREs) and indirectly associated with a range of alternative non-ERE elements. Interference with BRCA-1 expression and/or functions leads to high risk of breast or/and ovarian cancer. Our lab investigated the involvement of Human T-cell leukemia Virus Type 1 (HTLV-1) in breast cancer, since HTLV-1 Tax was found to strongly inhibit BRCA-1 expression. In addition, long exposure of 12-O-tetradecanoylphorbol-13-acetate (TPA), which is one of the stress-inducing agents activated the HTLV-1 promoter. So here the involvement of TPA in breast cancer had been examined by testing the effect of TPA on BRCA-1 and ERE expression. The results showed that TPA activated both BRCA-1 and ERE expression. In the 12 hours TPA activated the tow promoters more than others time, and after 24 hours the level of the tow promoters was decreased. Tax inhibited BRCA-1 expression but did not succeed to inhibit the effect of TPA. Then the activation of the two promoters was not through ERα pathway because TPA had no effect on ERα binding to the two promoters of the BRCA-1 and ERE. Also, the activation was not via nuclear factor kappa B (NF-κB) pathway because when the inhibitory of NF-κB had been added to the TPA, it still activated the tow promoters. However, it seems that 53BP1 may be involved in TPA activation of these promoters because ectopic high expression of 53BP1 significantly reduced the TPA activity. In addition, in the presence of Bisindolylmaleimide-I (BI)- the inhibitor of Protein Kinase C (PKC)- there was no activation for the two promoters, so the PKC is agonized BRCA-1 and ERE activation.

Keywords: BRCA-1, ERE, HTLV-1, TPA

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Authors: Mario Gómez, José Carlos Rodríguez

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This paper analyzes innovation trends in South Korea by means of the number of patent applications filed by residents and nonresidents during the period 1965 to 2012. Making use of patent data released by the World Intellectual Property Organization (WIPO), we search for the presence of multiple structural changes in patent application series in this country. These changes may suggest that firms’ innovative activity has been modified as a result of implementing some science, technology and innovation (STI) policies. Accordingly, the new regulations implemented in this country in the last decades have influenced its innovative activity. The question conducting this research is thus how STI policies in South Korea have influenced its innovation activity. The results confirm the existence of multiple structural changes in the series of patent applications resulting from alternative STI policies implemented during these years.

Keywords: econometric methods, innovation activity, Korea, patent applications, science, technology and innovation policy, STI

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Authors: Pui Shan Wong, Kosuke Tashiro, Satoru Kuhara, Sachiyo Aburatani

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Functional genomics and gene regulation inference has readily expanded our knowledge and understanding of gene interactions with regards to expression regulation. With the advancement of transcriptome sequencing in time-series comes the ability to study the sequential changes of the transcriptome. This method presented here works to augment existing regulation networks accumulated in literature with transcriptome data gathered from time-series experiments to construct a sequential representation of transcription factor activity. This method is applied on a time-series RNA-Seq data set from Escherichia coli as it transitions from growth to stationary phase over five hours. Investigations are conducted on the various metabolic activities in gene regulation processes by taking advantage of the correlation between regulatory gene pairs to examine their activity on a dynamic network. Especially, the changes in metabolic activity during phase transition are analyzed with focus on the pagP gene as well as other associated transcription factors. The visualization of the sequential transcriptional activity is used to describe the change in metabolic pathway activity originating from the pagP transcription factor, phoP. The results show a shift from amino acid and nucleic acid metabolism, to energy metabolism during the transition to stationary phase in E. coli.

Keywords: Escherichia coli, gene regulation, network, time-series

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Authors: Srisopa Ruangnoo, Arunporn Itharat

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The ethanolic and aqueous extracts of Parkia javanica Merr. germinating seeds and Parkia speciosa Hassk. seeds were evaluated for cytotoxic activity against three different types of human cancer cell lines including colon cancer (LS174T), breast cancer (MCF-7) and prostate cancer (PC3) using sulforhodamine B (SRB) assay. The fresh plant parts were divided into 2 parts. The first part was extracted by maceration with 95% ethanol for 3 days and then filtered, and the filtrates were evaporated by rotary evaporator. The other part was squeezed and filtered. Then the filtrates were dried by freeze dryer. The screening found that the aqueous extract of P. javanica Merr. germinating seeds exhibited more than 70% inhibition (at concentration 50 µg/ml) against all types of human cancer cells. The aqueous extract of P. javanica Merr. germinating seeds showed the highest cytotoxic activity against MCF-7 with the IC50 value as 5.63 µg/ml. The aqueous extract of P. javanica Merr. germinating seeds also showed high cytotoxic activity against PC3 and LS174T with the IC50 values as 10.79 and 11.40 µg/ml, respectively. In conclusion, P. javanica Merr. germinating seed is a natural source of anticancer activity and further research to isolate active compounds from this plant should be undertaken.

Keywords: cytotoxic activity, Parkia javanica Merr., Parkia speciosa Hassk., human cancer cell lines

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Authors: Ali Maksum

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In a number of countries, including Indonesia, the tendency for non-communicable diseases is increasing. As a result, health costs must be paid by the state continues to increase as well. People's lifestyles, including due to lack of physical activity, are thought to have contributed significantly to the problem. This study aims to examine the impact of participation in sports on quality of life, which is reflected in three main indicators, namely health, psychological, and social aspects. The study was conducted in the city of Surabaya and its surroundings, with a total of 490 participants, consisting of 245 men and 245 women with an average age of 45.4 years. Data on physical activity and quality of life were collected by questionnaire and analyzed using structural equation modeling. The test results of the model prove that the value of chi-square = 8,259 with p = .409, RMSEA = .008, NFI = .992, and CFI = 1. This means that the model is compatible with the data. The model explains that physical activity has a significant effect on quality of life. People who exercise regularly are better able to cope with stress, have a lower risk of illness, and have higher pro-social behavior. Therefore, it needs serious efforts from stakeholders, especially the government, to create an ecosystem that allows the growth of movement culture in the community.

Keywords: participation, physical activity, quality of life, structural equation modelling

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Authors: Hien Thi Thu Le, Nuno Rafael Candeias, Olli Yli-Harja, Meenakshisundaram Kandhavelu

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Purinergic receptor 1 (P2Y1R) is the potential therapeutic target for inducing prostate cancer (PCa) cell death. Recently, 1-indolinoalkyl 2-phenolic derivative, HIC, was identified as a P2Y1R agonist that increases apoptosis and inhibits cell proliferation of PCa. However, the biological effects of HIC have not been extensively studied at the molecular level. In the present study, we have investigated the anticancer effects of HIC and the molecular mechanisms underlying in PCa cells. Half maximal inhibitory concentration (IC₅₀) of HIC was measured as 15.98 μM and 15.64 μM for DU145 and PC3 cells, respectively. In addition, we found that HIC inhibited cell growth and metastasis of PC3 and DU145 cells colonies, spheroid areas, and migrated cells. RNA seq analysis revealed significant changes of over 3000 genes (p value < 0.05) upon HIC treatment in PC3 and DU145 cells. Genes involved in DNA damage, apoptosis, cell cycle arrest at G1/S phase were modulated by HIC treatment. MAPK and NF-κB protein array revealed the increased expression of ERK1/2, JNK1/2, p53 phosphorylation, and p53 protein. ERK1/2 and JNK1/2 activations are known to increase the stabilization of p53, a tumor suppressor protein, which is required to arrest the cell cycle at G1/S phase and cause cell death of PCa cells. Overall, our results suggest that HIC can serve as a multi-dimensional chemotherapeutic agent possessing strong cytotoxic, anti-cancer, and anti-metastasis against PCa growth.

Keywords: prostate cancer, P2Y1 receptor, apoptosis, metastasis

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Authors: Tripti Mishra, Shipra Shukla, Sanjeev Meena, , Ruchi Singh, Mahesh Pal, D. K. Upreti, Dipak Datta

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Roccella montagnei belongs to lichen family Roccelleceae growing luxuriantly along the coastal regions of India. As Roccella has been shown to be bioactive, we prepared methanolic extract and assessed its anticancer potential. The methanolic extract showed significant in vitro cytotoxic activity against four human cancer cell lines such as Colon (DLD-1, SW-620), Breast (MCF-7), Head and Neck (FaDu). This prompted us to isolate bioactive compounds through column chromatography. Two compounds Roccellic acid and Everninic acid have been isolated, out of which Everninic acid is reported for the first time. Both the compounds have been tested for in vitro cytotoxic activity in which Roccellic acid showed strong anticancer activity as compared to the Everninic acid. CDK-10 (Cyclin-dependent kinase) contributes to proliferation of cancer cells, and aberrant activity of these kinases has been reported in a wide variety of human cancers. These kinases, therefore, constitute biomarkers of proliferation and attractive pharmacological targets for the development of anticancer therapeutics. Therefore both the isolated compounds were tested for in silico molecular docking study against CDK-10 isomer enzyme to support the cytotoxic activity.

Keywords: cytotoxic activity, everninic acid, roccellic acid, R. montagnei

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Authors: Nikita Pasricha, Karen Smith, Simone Marshall, Vincent DePaul, Jessica Trier

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Understanding that physical activity in rehabilitation programs shapes outcomes in acquired brain injury (ABI) populations is not a new concept. However, there is a void in understanding the physical activity patterns of inpatients in ABI rehabilitation, the trajectory of physical activity recovery, and factors that contribute to the recovery of physical activity over the initial months post-ABI. The purpose of this study was to determine if physical activity patterns vary in people with recent ABI in inpatient rehabilitation. The study also investigated differences in physical activity patterns in ABI patients compared to age-related healthy participants. Results revealed that ABI patients spent approximately 6.7 times longer per day in sedentary postures than in active positions. In comparison, the control group spent only 2.8 times longer in sedentary postures compared to active positions. Patients with ABI took significantly fewer steps than age-matched health control participants. Within the ABI population, patients took 0.78 times fewer steps on weekends compared to weekdays. Participants with greater mobility limitations had a greater difference in WD to WE steps taken. Potential reasons could be from no structured weekend rehabilitation programs, lower availability of staff, or varying schedules. Given that the rehabilitation program is only structured on weekdays, further research to investigate the benefits of structured physical activities like group walking programs on weekends for ABI patients in inpatient rehabilitation programs is warranted.

Keywords: brain, ABI, TBI, rehabilitation

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Authors: Mohammad Kazem Mohammadi

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The use of anticancer agents forms an important part of the treatment of cancer of various types. Uranyl Complexes with DPHMP ligand have been used for the prevention and treatment of cancers. U(IV) metal complexes prepared by reaction of uranyl salt UO2 (NO3)2.6H2O with DPHMP in dry acetonitrile. Characterization of the ligand and its complexes was made by microanalyses, FT-IR, 1H NMR, 13C NMR and UV–Visible spectroscopy. These new complex showed excellent antitumor activity against two kinds of cancer cells that that are HT29:Haman colon adenocarcinoma cell line and T47D:human breast adenocarcinoma cell line.

Keywords: uranyl complexes, DPHMP ligand, antitumor activity, HT29, T47D

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Authors: Mokhtar Kouki Inès Rekik

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This paper focuses on the assessment of the air pollution and morbidity relationship in Tunisia. Air pollution is measured by ozone air concentration and the morbidity is measured by the number of respiratory-related restricted activity days during the 2-week period prior to the interview. Socioeconomic data are also collected in order to adjust for any confounding covariates. Our sample is composed by 407 Tunisian respondents; 44.7% are women, the average age is 35.2, near 69% are living in a house built after the 1980, and 27.8% have reported at least one day of respiratory-related restricted activity. The model consists on the regression of the number of respiratory-related restricted activity days on the air quality measure and the socioeconomic covariates. In order to correct for zero-inflation and heterogeneity, we estimate several models (Poisson, Negative binomial, Zero inflated Poisson, Poisson hurdle, Negative binomial hurdle and finite mixture Poisson models). Bootstrapping and post-stratification techniques are used in order to correct for any sample bias. According to the Akaike information criteria, the hurdle negative binomial model has the greatest goodness of fit. The main result indicates that, after adjusting for socioeconomic data, the ozone concentration increases the probability of positive number of restricted activity days.

Keywords: bootstrapping, hurdle negbin model, overdispersion, ozone concentration, respiratory-related restricted activity days

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Authors: Kartini Ilias, Nabilah Md Ahir, Nor Zafirah Ab Rahman, Safiah Md Yusof, Nuri Naqieyah Radzuan, Siti Sabariah Buhari

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This study aim to develop and assess the effectiveness of an intervention in improving eating habits and physical activity level of university students of UiTM Puncak Alam. The intervention consists of weekly dietary counselling by registered dietitian and high-intensity interval training (HIIT) for three times per week for the duration of 8 weeks. A total of 25 students from the intervention group and 25 students from control group who had BMI equal to or greater than 25kg/m² participated in the study. The results showed a significant reduction in body weight (3.0 kg), body fat percentage (7.9 %), waist circumference (7.3 cm) and BMI (2.9 kg/m²) between pre and post intervention. Besides, there was a significant increase in the level of physical activity among subjects in intervention group. In conclusion, the intervention made an impact on eating habit, physical activity level and improves weight status of the students. It is expected that the intervention could be adopted and implemented by the government and private sector as well as policy-makers in formulating obesity intervention.

Keywords: obesity, diet, obesity intervention, physical activity

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Authors: Vivek Singh Bhadauria, Abhishek Pandey

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Indole-2,3-diones are known for their various biological activities. By suitable control of a substituent, different novel indole-2,3-diones were synthesized. In this present study, various Schiff and Mannich bases were synthesized and characterized, and evaluated their for different pharmacological activities. The compounds were prepared by reacting indole-2,3-dione with benzyl chloride and 4-substituted thiosemicarbazides. All the synthesized compounds were characterized by the TLC, MP, Elemental analysis, FTIR, 1H-NMR and Mass spectroscopy. The compounds have been evaluated for their anticancer, antituberculosis, anticonvulsant, antiinflammatory as well as anti-SARS activity and the results are presented. Some of compounds possessed different pharmacological activity at a concentration of 200 mg/kg body weight and even at lower concentration.

Keywords: indoles, isatin, NMR, biological activities

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Authors: Mei-Fang Wu, Shu-Li Wang, Feng-Tsung Cheng

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Highly developed technology and highly competitive global market highlight the important role of competitive advantages and operation performances in sustainable company operation. Activity-Based Costing (ABC) provides accurate operation cost and operation performance information. Rich literature provide relevant research with cases study on Activity-Based Costing application, and yet, there is no research studying on cause relationship between key success factors of applying Activity-Based Costing and its specific outcomes, such as profitability or share market. These relationships provide the ways to handle the key success factors to achieve the specific outcomes for ensuring to promote the competitive advantages and operation performances. The main purposes of this research are exploring the key success paths by Key Success Paths approach which will lead the ways to apply Activity-Base Costing. The Key Success Paths is the innovative method which is exploring the cause relationships and explaining what are the effects of key success factors to specific outcomes of Activity-Based Costing implementation. The cause relationships between key success factors and successful specific outcomes are Key Success Paths (KSPs). KSPs are the guidelines to lead the cost management strategies to achieve the goals of competitive advantages and operation performances. The research findings indicate that good management system design may impact the good outcomes of Activity-Based Costing application and achieve to outstanding competitive advantage, operating performance and profitability as well by KSPs exploration.

Keywords: activity-based costing, key success factors, key success paths approach, key success paths, key failure paths

Procedia PDF Downloads 371

Authors: Chia-Hsun Chang

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Background: Combination of drug treatment, dietary management, and regular exercise can effectively control type II diabetes mellitus (T2DM). Performing daily physical activities other than structured exercise is much easier and whether daily physical activities including work, walking, housework, gardening, leisure exercise, or transportation have a similar effect on diabetes control is not well studied.Aims and Objectives: This study aims to determine whether daily physical activity undertaken by patients with T2DM is associated with their diabetes control. Design: A correlation study with prospective design. Methods: Purposive sampling of 206 patients with T2DM was recruited from a medical center in Central Taiwan. The International Physical Activity Questionnaire was used to assess daily levels of physical activities, and the Diabetes Compliance Questionnaire was used to assess medication and dietary compliance. Data of diabetes control (hemoglobin A1c, HbA1c)were followed up every three months for one year after recruitment. Results: In this study, the average age of the participants was 62.5 years (±10.4 years), and the average duration of diabetes since diagnosis was 13.2 years (±7.8), 112 of the participants were women (54.4%) and 94 of the participants were men (45.6%). The mean HbA1c level was 7.8% (±1.4), and 78.2% of the participants presented with unsatisfactory diabetes control. Because the participants were distributed across a wide age range, and their physical health, activity levels, and comorbidities might have varied with age, the participants were divided into two groups: 121 participants who were younger than 65 years (58.7%) and 85 participants who were older than 65 years (41.3%). Both younger (< 65 years) and older (> 65 years) patients with diabetes engaged in more moderate and low levels of physical activity (89.3% and 87%, respectively). Results showed that the levels of daily physical activity were not significantly associated with diabetes control after adjustment for medication and dietary compliance in both groups. Conclusion: Performing daily physical activity is not significantly correlated with diabetes control. Daily physical activity cannot completely replace exercise. Relevance to Clinical Practice: Health personnel must encourage patients to engage in exercise that is planned, structured, and repetitive for improving diabetes control.

Keywords: daily physical activity, diabetes control, international physical activity questionnaire (IPAQ), type II diabetes mellitus (T2DM)

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Authors: Young-Kwang Lee, Eun-Gu Ji, Min-Joo Kim, Seung-Jae Oh

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The purpose of this study is to develop a social participation activity scale for the elderly. As a result of exploratory factor analysis, confirmatory factor analysis was conducted using maximum likelihood method using bundled items. In conclusion, thirteen items of social participation activity scale seemed appropriate. Finally, convergent validity and discriminant validity were verified on the scale with the fit. The convergent validity was based on the variance extracted value. In other words, the hypothesis that the variables are the same is rejected and the validity is confirmed. This study extensively considered the measurement items of the social participation activity scale used to measure social participation activities of the elderly. In the future, it will be meaningful that it can be used as a tool to verify the effectiveness of services in organizations that provide social welfare services to elderly people such as comprehensive social welfare centers and the elderly comprehensive social welfare centers.

Keywords: elderly, social participation, scale development, validity

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Authors: Harish Rajak, Swati Singh

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A series of novel pyrimidine based semicarbazone were designed and synthesized on the basis of semicarbazone based pharmacophoric model to satisfy the structural prerequisite crucial for antiepileptic activity. The semicarbazones based pharmacophoric model consists of following four essential binding sites: (i) An aryl hydrophobic binding site with halo substituent; (ii) A hydrogen bonding domain; (iii) An electron donor group and (iv) Another hydrophobic-hydrophilic site controlling the pharmacokinetic features of the anticonvulsant. The aryl semicarbazones has been recognized as a structurally novel class of compounds with remarkable anticonvulsant activity. In the present study, all the test semicarbazones were subjected to molecular docking using Glide v5.8. Some of the compounds were found to interact with ARG192, GLU270 and THR353 residues of 1OHV protein, present in GABA-AT receptor. The chemical structures of the synthesized molecules were characterized by elemental and spectral (IR, 1H NMR, 13C NMR and MS) analysis. The anticonvulsant activities of the compounds were investigated using maximal electroshock seizure (MES) and subcutaneous pentylenetrtrazole (scPTZ) models. The neurotoxicity was evaluated in mice by the rotorod test. The attempts were also made to establish structure-activity relationships among synthesized compounds. The results of the present study confirmed that the pharmacophore model with four binding sites is essential for antiepileptic activity.

Keywords: pyrimidine, semicarbazones, anticonvulsant activity, neurotoxicity

Procedia PDF Downloads 237