Search results for: in vivo antimalarial activity

Authors: Nitin Jadhav, Pradeep R. Vavia

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Poor water soluble drugs are difficult to promote for oral drug delivery as they demonstrate poor and variable bioavailability because of its poor solubility and dissolution in GIT fluid. Nowadays lipid based formulations especially self microemulsifying drug delivery system (SMEDDS) is found as the most effective technique. With all the impressive advantages, the need of high amount of surfactant (50% - 80%) is the major drawback of SMEDDS. High concentration of synthetic surfactant is known for irritation in GIT and also interference with the function of intestinal transporters causes changes in drug absorption. Surfactant may also reduce drug activity and subsequently bioavailability due to the enhanced entrapment of drug in micelles. In chronic treatment these issues are very conspicuous due to the long exposure. In addition the liquid self microemulsifying system also suffers from stability issues. Recently one novel approach of solid stabilized micro and nano emulsion (Pickering emulsion) has very admirable properties such as high stability, absence or very less concentration of surfactant and easily converts into the dry form. So here we are exploring pickering dry emulsion system for dissolution enhancement of anti-lipemic, extremely poorly water soluble drug (Fenofibrate). Oil moiety for emulsion preparation was selected mainly on the basis of higher solubility of drug. Captex 300 was showed higher solubility for fenofibrate, hence selected as oil for emulsion. With Silica (solid stabilizer); Span 20 was selected to improve the wetting property of it. Emulsion formed by Silica and Span20 as stabilizer at the ratio 2.5:1 (silica: span 20) was found very stable at the particle size 410 nm. The prepared emulsion was further preceded for spray drying and formed microcapsule evaluated for in-vitro dissolution study, in-vivo pharmacodynamic study and characterized for DSC, XRD, FTIR, SEM, optical microscopy etc. The in vitro study exhibits significant dissolution enhancement of formulation (85 % in 45 minutes) as compared to plain drug (14 % in 45 minutes). In-vivo study (Triton based hyperlipidaemia model) exhibits significant reduction in triglyceride and cholesterol with formulation as compared to plain drug indicating increasing in fenofibrate bioavailability. DSC and XRD study exhibit loss of crystallinity of drug in microcapsule form. FTIR study exhibit chemical stability of fenofibrate. SEM and optical microscopy study exhibit spherical structure of globule coated with solid particles.

Keywords: captex 300, fenofibrate, pickering dry emulsion, silica, span20, stability, surfactant

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Authors: Maxime Moreau, Silvère Baron, Jean-Marc Lobaccaro, Karine Charlet, Sébastien Menecier, Frédéric Perisse

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Cold Atmospheric Plasma (CAP) is an ionized gas generated at atmospheric pressure with the temperature of heavy particles (molecules, ions, atoms) close to the room temperature. Recent studies have shown that both in-vitro and in-vivo plasma exposition to many cancer cell lines are efficient to induce the apoptotic way of cell death. In some other works, normal cell lines seem to be less impacted by plasma than cancer cell lines. This is called selectivity of plasma. It is highly likely that the generated RNOS (Reactive Nitrogen Oxygen Species) in the plasma jet, but also in the medium, play a key-role in this selectivity. In this study, two CAP devices will be compared to electrical power, chemical species composition and their efficiency to kill cancer cells. A particular focus on the action of hydrogen peroxide will be made. The experiments will take place as described next for both devices: electrical and spectroscopic characterization for different voltages, plasma treatment of normal and cancer cells to compare the CAP efficiency between cell lines and to show that death is induced by an oxidative stress. To enlighten the importance of hydrogen peroxide, an inhibitor of H2O2 will be added in cell culture medium before treatment and a comparison will be made between the results of cell viability in this case and those from a simple plasma exposition. Besides, H2O2 production will be measured by only treating medium with plasma. Cell lines will also be exposed to different concentrations of hydrogen peroxide in order to characterize the cytotoxic threshold for cells and to make a comparison with the quantity of H2O2 produced by CAP devices. Finally, the activity of catalase for different cell lines will be quantified. This enzyme is an important antioxidant agent against hydrogen peroxide. A correlation between cells response to plasma exposition and this activity could be a strong argument in favor of the predominant role of H2O2 to explain the selectivity of plasma cancer treatment by cold atmospheric plasma.

Keywords: cold atmospheric plasma, hydrogen peroxide, prostate cancer, selectivity

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Authors: Bright Chukwunwike Uzuegbunam, Wojciech Paslawski, Hans Agren, Christer Halldin, Wolfgang Weber, Markus Luster, Thomas Arzberger, Behrooz Hooshyar Yousefi

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There is a need to develop a PET tracer that will enable to diagnosis and track the progression of Alpha-synucleinopathies (Parkinson’s disease [PD], dementia with Lewy bodies [DLB], multiple system atrophy [MSA]) in living subjects over time. Alpha-synuclein aggregates (a-syn), which are present in all the stages of disease progression, for instance, in PD, are a suitable target for in vivo PET imaging. For this reason, we have developed some promising a-syn tracers based on a disarylbisthiazole (DABTA) scaffold. The precursors are synthesized via a modified Hantzsch thiazole synthesis. The precursors were then radiolabeled via one- or two-step radiofluorination methods. The ligands were initially screened using a combination of molecular dynamics and quantum/molecular mechanics approaches in order to calculate the binding affinity to a-syn (in silico binding experiments). Experimental in vitro binding assays were also performed. The ligands were further screened in other experiments such as log D, in vitro plasma protein binding & plasma stability, biodistribution & brain metabolite analyses in healthy mice. Radiochemical yields were up to 30% - 72% in some cases. Molecular docking revealed possible binding sites in a-syn and also the free energy of binding to those sites (-28.9 - -66.9 kcal/mol), which correlated to the high binding affinity of the DABTAs to a-syn (Ki as low as 0.5 nM) and selectivity (> 100-fold) over Aβ and tau, which usually co-exist with a-synin some pathologies. The log D values range from 2.88 - 2.34, which correlated with free-protein fraction of 0.28% - 0.5%. Biodistribution experiments revealed that the tracers are taken up (5.6 %ID/g - 7.3 %ID/g) in the brain at 5 min (post-injection) p.i., and cleared out (values as low as 0.39 %ID/g were obtained at 120 min p.i. Analyses of the mice brain 20 min p.i. Revealed almost no radiometabolites in the brain in most cases. It can be concluded that in silico study presents a new venue for the rational development of radioligands with suitable features. The results obtained so far are promising and encourage us to further validate the DABTAs in autoradiography, immunohistochemistry, and in vivo imaging in non-human primates and humans.

Keywords: alpha-synuclein aggregates, alpha-synucleinopathies, PET imaging, tracer development

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Authors: Sanja O. Podunavac-Kuzmanović, Strahinja Z. Kovačević, Lidija R. Jevrić, Stela Jokić

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The subject of this paper is to correlate antibacterial behavior of benzimidazole derivatives with their molecular characteristics using chemometric QSAR (Quantitative Structure–Activity Relationships) approach. QSAR analysis has been carried out on the inhibitory activity of benzimidazole derivatives against Staphylococcus aureus. The data were processed by linear least squares (LLS) and artificial neural network (ANN) procedures. The LLS mathematical models have been developed as a calibration models for prediction of the inhibitory activity. The quality of the models was validated by leave one out (LOO) technique and by using external data set. High agreement between experimental and predicted inhibitory acivities indicated the good quality of the derived models. These results are part of the CMST COST Action No. CM1306 "Understanding Movement and Mechanism in Molecular Machines".

Keywords: Antibacterial, benzimidazoles, chemometric, QSAR.

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Authors: P.P. Rupasinghe, A.H. Farid

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The Aleutian mink disease virus (AMDV, Carnivore amdoparvovirus 1) causes persistent infection, plasmacytosis, and formation and deposition of immune complexes in various organs in adult mink, leading to glomerulonephritis, arteritis and sometimes death. The disease has no cure nor an effective vaccine, and identification and culling of mink positive for anti-AMDV antibodies have not been successful in controlling the infection in many countries. The failure to eradicate the virus from infected farms may be caused by keeping false-negative individuals on the farm, virus transmission from wild animals, or neighboring farms. The identification of sources of infection, which can be performed by comparing viral sequences, is important in the success of viral eradication programs. High mutation rates could cause inaccuracies when viral sequences are used to trace back an infection to its origin. There is no published information on the mutation rate of AMDV either in vivo or in vitro. The in vivo estimation is the most accurate method, but it is difficult to perform because of the inherent technical complexities, namely infecting live animals, the unknown numbers of viral generations (i.e., infection cycles), the removal of deleterious mutations over time and genetic drift. The objective of this study was to determine the mutation rate of AMDV on which no information was available. A homogenate was prepared from the spleen of one naturally infected American mink (Neovison vison) from Nova Scotia, Canada (parental template). The near full-length genome of this isolate (91.6%, 4,143 bp) was bidirectionally sequenced. A group of black mink was inoculated with this homogenate (descendant mink). Spleen sampled were collected from 10 descendant mink after 16 weeks post-inoculation (wpi) and from anther 10 mink after 176 wpi, and their near-full length genomes were bi-directionally sequenced. Sequences of these mink were compared with each other and with the sequence of the parental template. The number of nucleotide substitutions at 176 wpi was 3.1 times greater than that at 16 wpi (113 vs 36) whereas the estimates of mutation rate at 176 wpi was 3.1 times lower than that at 176 wpi (2.85×10-3 vs 9.13×10-4 substitutions/ site/ year), showing a decreasing trend in the mutation rate per unit of time. Although there is no report on in vivo estimate of the mutation rate of DNA viruses in animals using the same method which was used in the current study, these estimates are at the higher range of reported values for DNA viruses determined by various techniques. These high estimates are logical based on the wide range of diversity and pathogenicity of AMDV isolates. The results suggest that increases in the number of nucleotide substitutions over time and subsequent divergence make it difficult to accurately trace back AMDV isolates to their origin when several years elapsed between the two samplings.

Keywords: Aleutian mink disease virus, American mink, mutation rate, nucleotide substitution

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Authors: Rajesh Kumar, Anil Kamboj

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Inhibition of α- amylase play a vital role in the clinical management of postprandial hyperglycemia. Although, powerful synthetic inhibitors are available, natural inhibitors are potentially safer. The present study was carried out to evaluate α- amylase inhibition activity from hydroalcoholic extracts from aerial parts of Cestrum nocturnum. Hydroalcoholic extract was prepared by Soxhletation Method. The extract showed strong inhibition towards α- amylase activity and IC50 value were 45.9 µg. This In vitro studies indicate the potential of C. nocturnum in the development of effective anti-diabetic agents.

Keywords: α- amylase, cestrum nocturnum, hyperglycemia, hydroalcoholic extracts, diabetes

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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: Gulnur Arabaci

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Heavy metals are one of the major groups of contaminants in the environment and many of them are toxic even at very low concentration in plants and animals. However, some metals play important roles in the biological function of many enzymes in living organisms. Metals such as zinc, iron, and cooper are important for survival and activity of enzymes in plants, however heavy metals can inhibit enzyme which is responsible for defense system of plants. Polyphenol oxidase (PPO) is a copper-containing metalloenzyme which is responsible for enzymatic browning reaction of plants. Enzymatic browning is a major problem for the handling of vegetables and fruits in food industry. It can be increased and effected with many different futures such as metals in the nature and ground. In the present work, PPO was isolated and characterized from green leaves of red poppy plant (Papaver rhoeas). Then, the effect of some known antibrowning agents which can form complexes with metals and metals were investigated on the red poppy PPO activity. The results showed that glutathione was the most potent inhibitory effect on PPO activity. Cu(II) and Fe(II) metals increased the enzyme activities however, Sn(II) had the maximum inhibitory effect and Zn(II) and Pb(II) had no significant effect on the enzyme activity. In order to reduce the effect of heavy metals, the effects of metal-antibrowning agent complexes on the PPO activity were determined. EDTA and metal complexes had no significant effect on the enzyme. L-ascorbic acid and metal complexes decreased but L-ascorbic acid-Cu(II)-complex had no effect. Glutathione–metal complexes had the best inhibitory effect on Red poppy leaf PPO activity.

Keywords: inhibition, metal, red poppy, poly phenol oxidase (PPO)

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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: Zerihun Tesfaye Nigusse

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Objective: This study evaluates the antileishmanial activity of the methanolic extract of Aloe otallensis (A. otallensis) on the promastigote stage of Leishmaniadonovani (L. donovani) as compared to standard drugs and to screen its phytochemical constituents. Methods: Phytochemical screening was done by using the method mentioned by Evans and Trease on methanolic extract of the exudates of Aloe otallensis leaves. The extract was also evaluated for in vitro antileishmanial activity against L. donavani, which is found in the Parasitology Unit of Black Lion Hospital. The result was compared to standard drugs of sodium stibogluconate, milfostin and paramomycin. Results: The extract has good antileishmanial activity with an IC50 of 0.123 0 μg/mL on L. donovani (AM 563). The experimental data showed that relatively, it had better activity than paramomycin and milfostin but less activity than sodium stibogluconate. The data analyses were done by GraphPad Prism version 5 software after it was read by an ELISA reader at the wavelength of 650 nm. The phytochemical screening of the exudates of A. otallensis showed the presence of phenol, alkaloid and saponin. Conclusions: The methanol extract of the exudates of A.otallensishas a good anti- leishmaniasis activity and this may be attributed to phenol, alkaloid and saponin present in the plant. But it needs further analysis for the conformation of which constituent presents in high concentration to know which one has the strongest effect.

Keywords: anti leshimaniasis, aloe otallensis, leshimania ethiopica, IC50

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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: Puchita Chokcharoenying

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Polyphenols are the most abundant antioxidants found in plants, and they are highly effective at scavenging oxidative free radicals. Antioxidants are substances found in medicinal plants to help prevent heart disease, stroke, and some cancers. This study focused on evaluating the flavonoids content of Chrysanthemum Indicum and determine their antioxidant capacity by using DPPH and ABTS radical scavenging capacity assay. The total flavonoid content of C. indicumextract was determined and expressed as quercetin equivalents (QE)/g measured by an aluminiumchloride colorimetric method. The results showed that the IC50 of C. indicum extract were 83.57μg/mL ± 0.875 and52.57μg/mL ± 0.632for DPPH and ABTS, respectively. C. indicumextract exhibited antioxidant activities as a concentration dependent manner. In the DPPH assay, vitamin C was used as a positive control, whereas Trolox was used as a positive control in the ABTS assay. In summary, C. indicum extract is rich in flavonoids, which have potent antioxidant properties. Thus, C. indicum extract is a good source of antioxidants and can be developed for medicinal purposes. Nevertheless, more research on the antioxidant activity of C. indicum extract and in vivo antioxidant studies are still needed.

Keywords: ABTS assay, antioxidant, chrysanthemum indicum, DPPH assay, total flavonoid content

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Authors: Bhavini Patel, Aslihan Ugun-Klusek, Ellen Billet

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The two main contributing factors to familial and idiopathic form of Parkinson’s disease (PD) are oxidative stress and altered proteolysis. Monoamine oxidase-A (MAO-A) plays a significant role in redox homeostasis by producing reactive oxygen species (ROS) via deamination of for example, dopamine. The ROS generated induces chemical modification of proteins resulting in altered biological function. The ubiquitin-proteasome system, which consists of three different types or proteolytic activity, namely “chymotrypsin-like” activity (CLA), “trypsin-like” activity (TLA) and “post acidic-like” activity (PLA), is responsible for the degradation of ubiquitinated proteins. Defects in UPS are known to be strongly correlated to PD. Herein, the effect of ROS generated by MAO-A on proteasome activity and the effects of proteasome inhibition on MAO-A protein levels in WT, mock and MAO-A overexpressed (MAO-A+) SHSY5Y neuroblastoma cell lines were investigated. The data in this study report increased proteolytic activity when MAO-A protein levels are significantly increased, in particular CLA and PLA. Additionally, 20S proteasome inhibition induced a decrease in MAO-A levels in WT and mock cells in comparison to MAO-A+ cells in which 20S proteasome inhibition induced increased MAO-A levels to be further increased at 48 hours of inhibition. This study supports the fact that MAO-A could be a potential pharmaceutical target for neuronal protection as data suggests that endogenous MAO-A levels may be essential for modulating cell death and survival.

Keywords: monoamine oxidase, neurodegeneration, Parkinson's disease, proteasome

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Authors: Strahinja Z. Kovačević, Lidija R. Jevrić, Sanja O. Podunavac Kuzmanović

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The relationship between antibacterial activity of eighteen different substituted benzimidazole derivatives and their molecular characteristics was studied using chemometric QSAR (Quantitative Structure–Activity Relationships) approach. QSAR analysis has been carried out on inhibitory activity towards Staphylococcus aureus, by using molecular descriptors, as well as minimal inhibitory activity (MIC). Molecular descriptors were calculated from the optimized structures. Principal component analysis (PCA) followed by hierarchical cluster analysis (HCA) and multiple linear regression (MLR) was performed in order to select molecular descriptors that best describe the antibacterial behavior of the compounds investigated, and to determine the similarities between molecules. The HCA grouped the molecules in separated clusters which have the similar inhibitory activity. PCA showed very similar classification of molecules as the HCA, and displayed which descriptors contribute to that classification. MLR equations, that represent MIC as a function of the in silico molecular descriptors were established. The statistical significance of the estimated models was confirmed by standard statistical measures and cross-validation parameters (SD = 0.0816, F = 46.27, R = 0.9791, R2CV = 0.8266, R2adj = 0.9379, PRESS = 0.1116). These parameters indicate the possibility of application of the established chemometric models in prediction of the antibacterial behaviour of studied derivatives and structurally very similar compounds.

Keywords: antibacterial, benzimidazole, molecular descriptors, QSAR

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Authors: Michael Graz, Andrew Shearer, Gareth Evans

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Manipulation of rumen bacteria is receiving increasing attention as a way of controlling greenhouse gas (GHG) emissions that are generated by the agricultural sector. Feed supplementation in particular is one of the ways in which this drive is being addressed, in particular with reference to livestock-generated GHG emissions. A blend of naturally occurring chemical extracts obtained from garlic and bitter orange extracts has been identified as a natural, sustainable and non-antibiotic based way of reducing methane production by ruminant livestock. In the current study, the acceptability and impact of this blend of natural extracts on feed rations of beef cattle was trialed in vivo on a commercial farm in Europe. Initial findings have demonstrated acceptable palatability, with all animals accepting the feed supplement into their ration both when it was mixed into the total daily ration and when used as a part of their high energy rations. Measurement of the impact of this feed supplement on productivity weight gain and milk quality is ongoing. In conclusion, this field study confirmed the palatability of the combination of garlic and citrus extracts and hence pointed to possibility of the extract blend to improve digestion, enhance body energy retention and limit CH4 formation in relation to feed intake.

Keywords: citrus, garlic, methane reduction, palatability, ruminants

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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: Sanjay Shukla

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Excessive use of antibiotics is a main problem in the treatment of wounds and other chronic infections and antibiotic treatment is frequently non-curative, thus alternative treatment is necessary. Phage therapy is considered one of the most effective approaches to treat multi-drug resistant bacterial pathogens. Infections caused by Staphylococcus aureus are very efficiently controlled with phage cocktails, containing a different individual phages lysate infecting a majority of known pathogenic S. aureus strains. The aim of current study was to investigate the efficiency of a purified phage cocktail for prophylactic as well as therapeutic application in mouse model and in large animals with chronic septic infection of wounds. A total of 150 sewage samples were collected from various livestock farms. These samples were subjected for the isolation of bacteriophage by double agar layer method. A total of 27 sewage samples showed plaque formation by producing lytic activity against S. aureus in double agar overlay method out of 150 sewage samples. In TEM recovered isolates of bacteriophages showed hexagonal structure with tail fiber. In the bacteriophage (ØVS) had an icosahedral symmetry with the head size 52.20 nm in diameter and long tail of 109 nm. Head and tail were held together by connector and can be classified as a member of the Myoviridae family under the order of Caudovirale. Recovered bacteriophage had shown the antibacterial activity against the S. aureus in vitro. Cocktail (ØVS1, ØVS5, ØVS9 and ØVS 27) of phage lysate were tested to know in vivo antibacterial activity as well as the safety profile. Result of mice experiment indicated that the bacteriophage lysate was very safe, did not show any appearance of abscess formation which indicates its safety in living system. The mice were also prophylactically protected against S. aureus when administered with cocktail of bacteriophage lysate just before the administration of S. aureus which indicates that they are good prophylactic agent. The S. aureus inoculated mice were completely recovered by bacteriophage administration with 100% recovery which was very good as compere to conventional therapy. In present study ten chronic cases of wound were treated with phage lysate and follow up of these cases was done regularly up to ten days (at 0, 5 and 10 d). Result indicated that the six cases out of ten showed complete recovery of wounds within 10 d. The efficacy of bacteriophage therapy was found to be 60% which was very good as compared to the conventional antibiotic therapy in chronic septic wounds infections. Thus, the application of lytic phage in single dose proved to be innovative and effective therapy for treatment of septic chronic wounds.

Keywords: phage therapy, phage lysate, antimicrobial resistance, S. aureus

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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: 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: Kais Rtibi, Slimen Selmi, Jamel El-Benna, Lamjed Marzouki, Hichem Sebai

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Background: Myeloperoxidase (MPO) is a hemic enzyme found in high concentrations in the primary neutrophils granules. In addition to its peroxidase activity, it has a chlorination activity, using hydrogen peroxide and chloride ions to form hypochlorous acid, a strong oxidant, capable of chlorinating molecules. Bioactive compounds contained in medicinal plants could limit the action of this enzyme to reduce the reactive oxygen species production and its chlorination activity. The purpose of this study is to evaluate the effect of the carob aqueous extract (CAE) on the release of MPO by human neutrophils in vitro and its activity following stimulation of these cells by PMA. Methods: Neutrophils were isolated by simple sedimentation using the Dextran/Ficoll method. After stimulation with phorbol 12-myristate 13-acetate (PMA), neutrophils release the MPO by degranulation. The effect of CAE on the release of MPO was analyzed by the Western blot technique, while, its activity was determined by biochemical method using the method of 3,3', 5,5'- Tetramethylbenzidine (TMB) and hydrogen peroxide. The data were expressed as mean ± SEM. Results: The carob aqueous extract causes a decrease in MPO quantity and activity in a concentration-dependent manner which leads to a reduction of the production of the ROS (reactive oxygen species) and the protection of the molecules against oxidation and chlorination mechanisms. Conclusion: Thanks to its richness in bioactive compounds, the aqueous extract of carob could limit the development of damages related to the uncontrolled activity of MPO.

Keywords: carob, MPO, myeloperoxidase, neutrophils, PMA, phorbol 12-myristate 13-acetate

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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: Yik Ling Chew, Adlina Maisarah Mahadi, Joo Kheng Goh

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Bauhinia kockiana originates from Peninsular Malaysia, and it is grown as a garden ornamental plant. However, it is used as medicinal plant by Malaysia ‘Kelabit’ ethic group in treating various diseases and illnesses. This study focused on the assessment of the antibacterial activity of B. kockiana towards MRSA, to purify and identify the antibacterial compounds, and to determine the mechanism of antibacterial activity. Antibacterial activity of B. kockiana flower is evaluated qualitatively and quantitatively using disc diffusion assay and microbroth dilution method to determine the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of extracts. Phytochemical analysis is performed to determine the classes of phytochemicals in the extracts. Bioactivity-guided isolation is performed to purify the antibacterial agents and identified the chemical structures via various spectroscopy methods. Scanning electron microscopy (SEM) technique is adopted to evaluate the antibacterial mechanism of extract and compounds isolated. B. kockiana flower is found to exhibit fairly strong antibacterial activity towards both strains of MRSA bacteria. Gallic acid and its ester derivatives are purified from ethyl acetate extract and the antibacterial activity is evaluated. SEM has revealed the mechanism of the extracts and compounds isolated.

Keywords: alkyl gallates, Bauhinia kockiana, MRSA, scanning electron microscopy

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Authors: Maryam Zahedifard, Fadhil Lafta Faraj, Nazia Abdul Majid, Hapipah Mohd Ali, Mahmood Ameen Abdulla

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The new quinazoline Schiff bases have been synthesized through condensation reaction of 2-aminobenzhydrazide with 5-bromosalicylaldehyde and 3-methoxy-5-bromosalicylaldehyde. The compound was investigated for anticancer activity against MCF-7 human breast cancer cell line. It demonstrated a remarkable antiproliferative effect, with an IC50 value of 3.41±0.34, after 72 hours of treatment. Most apoptosis morphological features in treated MCF-7 cells were observed by AO/PI staining. The results of cell cycle analysis indicate that compounds did not induce S and M phase arrest in cell after 24 hours of treatment. Furthermore, MCF-7 cells treated with compound subjected to apoptosis death, as exhibited by perturbation of mitochondrial membrane potential and cytochrome C release as well as increase in ROS generation. We also found activation of caspases 3/7 and -9. Moreover, acute toxicity results demonstrated the nontoxic nature of the compounds in mice. Our results showed the selected compound significantly induce apoptosis in MCF-7 cells via intrinsic pathway, which might be considered as a potential candidate for further in vivo and clinical breast cancer studies.

Keywords: quinazoline Schiff base, apoptosis, MCF-7, caspase, cell cycle, acute toxicity

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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

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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

Procedia PDF Downloads 189