Search results for: uncompetitive inhibition.
Commenced in January 2007
Frequency: Monthly
Edition: International
Paper Count: 140

Search results for: uncompetitive inhibition.

50 The Antimicrobial Activity of the Essential Oil of Salvia officinalis Harvested in Boumerdes

Authors: N. Meziou-Chebouti, A. Merabet, N. Behidj, F-Z. Bissaad

Abstract:

The Algeria by its location offers a rich and diverse vegetation. A large number of aromatic and medicinal plants grow spontaneously. The interest in these plants has continued to grow in recent years. Their particular properties due to the essential oil fraction can be utilized to treat microbial infections. To this end, and in the context of the valuation of the Algerian flora, we became interested in the species of the family Lamiaceae which is one of the most used as a global source of spices. The plant on which we have based our choice is a species of sage "Salvia officinalis" from the Isser localized region within the province of Boumerdes. This work focuses on the study of the antimicrobial activity of essential oil extracted from the leaves of Salvia officinalis. The extraction is carried out by essential oil hydrodistillation and reveals a yield of 1.06℅. The study of the antimicrobial activity of the essential oil by the method of at aromatogramme shown that Gram positive bacteria are most susceptible (Staphylococcus aureus and Bacillus subtilis) with a strong inhibition of growth. The yeast Candida albicans fungus Aspergillus niger and have shown moderately sensitive.

Keywords: Aromatogram, anti-microbial activity, essential oil, Salvia officinalis.

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49 In vivo Therapeutic Potential of Biologically Synthesized Silver Nanoparticles

Authors: Kalakotla Shanker, G. Krishna Mohan

Abstract:

Nowadays, nanoparticles are being used in pharmacological studies for their exclusive properties such as small size, more surface area, biocompatibility and enhanced solubility. In view of this, the present study aimed to evaluate the antihyperglycemic potential of biologically synthesized silver nanoparticles (BSSNPs) and Gymnema sylvestre (GS) extract. The SEM and SEM analysis divulges that the BSSNPs were spherical in shape. EDAX spectrum exhibits peaks for the presence of silver, carbon, and oxygen atoms in the range of 1.0-3.1 keV. FT-IR reveals the binding properties of active bio-constituents responsible for capping and stabilizing BSSNPs. The results showed increased blood glucose, huge loss in body weight and downturn in plasma insulin. The GS extract (200 mg/kg, 400 mg/kg), BSSNPs (100 mg/kg, 200 mg/kg) and metformin 50 mg/kg were administered to the diabetic rats. BSSNPs at a dose level of 200 mg/kg (b.wt.p.o.) showed significant inhibition of (p<0.001) blood glucose levels as compared with GS extract treated group. The results obtained from study indicate that the BSSNP shows potent anti-diabetic activity.

Keywords: BSSNP, G.sylvetre, wistar rats, antihyperglycemic activity.

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48 Hypothesis of a Holistic Treatment of Cancer: Crab Method

Authors: Devasis Ghosh

Abstract:

The main hindrance to total cure of cancer is a) the failure to control continued production of cancer cells, b) its sustenance and c) its metastasis. This review study has tried to address this issue of total cancer cure in a more innovative way. A 10-pronged “CRAB METHOD”, a novel holistic scientific approach of Cancer treatment has been hypothesized in this paper. Apart from available Chemotherapy, Radiotherapy and Oncosurgery, (which shall not be discussed here), seven other points of interference and treatment has been suggested, i.e. 1. Efficient stress management. 2. Dampening of ATF3 expression. 3. Selective inhibition of Platelet Activity. 4. Modulation of serotonin production, metabolism and 5HT receptor antagonism. 5. Auxin, its anti-proliferative potential and its modulation. 6. Melatonin supplementation because of its oncostatic properties. 7. HDAC Inhibitors especially valproic acid use due to its apoptotic role in many cancers. If all the above stated seven steps are thoroughly taken care of at the time of initial diagnosis of cancer along with the available treatment modalities of Chemotherapy, Radiotherapy and Oncosurgery, then perhaps, the morbidity and mortality rate of cancer may be greatly reduced.

Keywords: ATF3 dampening, auxin modulation, cancer, platelet activation, serotonin, stress, valproic acid.

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47 Progressive Loading Effect of Co over SiO2/Al2O3 Catalyst for Cox Free Hydrogen and Carbon Nanotubes Production via Catalytic Decomposition of Methane

Authors: Sushil Kumar Saraswat, K. K. Pant

Abstract:

Co metal supported on SiO2 and Al2O3 catalysts with a metal loading varied from 30 of 70 wt.% were evaluated for decomposition of methane to COx free hydrogen and carbon nanomaterials. The catalytic runs were carried out from 550-800oC under atmospheric pressure using fixed bed vertical flow reactor. The fresh and spent catalysts were characterized by BET surface area analyzer, XRD, SEM, TEM and TG analysis. The data showed that 50% Co/Al2O3 catalyst exhibited remarkable higher activity at 800oC with respect to H2 production compared to rest of the catalysts. However, the catalytic activity and durability was greatly declined at higher temperature. The main reason for the catalytic inhibition of Co containing SiO2 catalysts is the higher reduction temperature of Co2SiO4. TEM images illustrate that the carbon materials with various morphologies, carbon nanofibers (CNFs), helical-shaped CNFs and branched CNFs depending on the catalyst composition and reaction temperature were obtained.

Keywords: Carbon nanotubes, Cobalt, Hydrogen Production, Methane decomposition.

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46 A Model for Test Case Selection in the Software-Development Life Cycle

Authors: Adtha Lawanna

Abstract:

Software maintenance is one of the essential processes of Software-Development Life Cycle. The main philosophies of retaining software concern the improvement of errors, the revision of codes, the inhibition of future errors, and the development in piece and capacity. While the adjustment has been employing, the software structure has to be retested to an upsurge a level of assurance that it will be prepared due to the requirements. According to this state, the test cases must be considered for challenging the revised modules and the whole software. A concept of resolving this problem is ongoing by regression test selection such as the retest-all selections, random/ad-hoc selection and the safe regression test selection. Particularly, the traditional techniques concern a mapping between the test cases in a test suite and the lines of code it executes. However, there are not only the lines of code as one of the requirements that can affect the size of test suite but including the number of functions and faulty versions. Therefore, a model for test case selection is developed to cover those three requirements by the integral technique which can produce the smaller size of the test cases when compared with the traditional regression selection techniques.

Keywords: Software maintenance, regression test selection, test case.

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45 A Model for Test Case Selection in the Software-Development Life Cycle

Authors: Adtha Lawanna

Abstract:

Software maintenance is one of the essential processes of Software-Development Life Cycle. The main philosophies of retaining software concern the improvement of errors, the revision of codes, the inhibition of future errors, and the development in piece and capacity. While the adjustment has been employing, the software structure has to be retested to an upsurge a level of assurance that it will be prepared due to the requirements. According to this state, the test cases must be considered for challenging the revised modules and the whole software. A concept of resolving this problem is ongoing by regression test selection such as the retest-all selections, random/ad-hoc selection and the safe regression test selection. Particularly, the traditional techniques concern a mapping between the test cases in a test suite and the lines of code it executes. However, there are not only the lines of code as one of the requirements that can affect the size of test suite but including the number of functions and faulty versions. Therefore, a model for test case selection is developed to cover those three requirements by the integral technique which can produce the smaller size of the test cases when compared with the traditional regression selection techniques.

Keywords: Software maintenance, regression test selection, test case.

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44 Prevalence and Fungicidal Activity of Endophytic Micromycetes of Plants in Kazakhstan

Authors: L. V. Ignatova, Y. V. Brazhnikova, T. D. Mukasheva, R. Zh. Berzhanova, A. A. Omirbekova

Abstract:

Endophytic microorganisms are presented in plants of different families growing in the foothills and piedmont plains of Trans-Ili Alatau. It was found that the maximum number of endophytic micromycetes is typical to the Fabaceae family. The number of microscopic fungi in the roots reached (145.9±5.9)×103 CFU/g of plant tissue; yeasts - (79.8±3.5)×102 CFU/g of plant tissue. Basically, endophytic microscopic fungi are typical for underground parts of plants. In contrast, yeasts more infected aboveground parts of plants. Small amount of micromycetes is typical to inflorescence and fruits. Antagonistic activity of selected micromycetes against Fusarium graminearum, Cladosporium sp., Phytophtora infestans and Botrytis cinerea phytopathogens was detected. Strains with a broad, narrow and limited range of action were identified. For further investigations Rh2 and T7 strains were selected, they are characterized by a broad spectrum of fungicidal activity and they formed the large inhibition zones against phytopathogens. Active antagonists are attributed to the Rhodotorula mucilaginosa and Beauveria bassiana species.

Keywords: Endophytic micromycetes, fungicidal activity, prevalence.

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43 Study on Nitrite Accumulation Characteristics and Nitrifying Population Dynamics at Different Growth Environments

Authors: Yunxia Zhang, Jiti Zhou, Jianbo Guo, Xiuhong Zhang, Lihong Zhao, Shouzhi Yuan

Abstract:

Novel nitrogen removal technologies via nitrite pathway attract increasing interest in recent years. In this study, batch experiments were performed to investigate nitrite accumulation characteristics and shifts in nitrifying community structure at different growth environments including ammonia concentration, pH and alkalinity. It was found that nitrite accumulation ratios were maintained at around 95% at studied conditions, and the optimum pH and Alk/N (ratio between alkalinity and nitrogen) for ammonium oxidization were 8.5 and 8.33, respectively. Fluorescence in situ hybridization analysis of nitrifying bacteria showed that high free ammonia (from influent ammonium or caused by high pH) significantly altered the structure of nitrifying community, leading to abundance of ammonia-oxidizing bacteria (AOB), especially Nitrososmonas, and inhibition of nitrite-oxidizing bacteria (NOB). The results suggest that free ammonia plays more important role than other studied conditions on nitrite accumulation.

Keywords: Partial nitrification, Nitrite accumulation, Nitrifyingbacteria, Fluorescence in situ hybridization (FISH).

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42 Formulation and Characterization of Drug Loaded Niosomal Gel for Anti-Inflammatory Activity

Authors: Sunil Kamboj, Vipin Saini, Suman Bala, Gaurav Sharma

Abstract:

The main aim of the present research was to encapsulate mefenamic acid in niosomes andincorporate the prepared niosomes in the carbopol gel base for sustained therapeutic action. Mefenamic acid loaded niosomes were prepared by thin film hydration technique and evaluated for entrapment efficiency, vesicular size and zeta potential. The entrapment efficiency of the prepared niosomes was found to increase with decreasing the HLB values of surfactants and vesicle size was found to increase with increasing the cholesterol concentration. Niosomal vesicles with good entrapment efficiencies were incorporated in carbopol gel base to form the niosomal gel. The prepared niosomal gel was evaluated for pH, viscosity, spreadability, extrudability and skin permeation study across the rat skin. The results of permeation study revealed that the gel formulated with span 60 niosomes sustained the drug release for 12h. Further the in vivo study showed the good inhibition of inflammation by the gel prepared with span 60 niosomes.

Keywords: Mefenamic acid, niosomal gel, nonionic surfactants, sustained release.

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41 Effectiveness of the Flavonoids Isolated from Thymus inodorus by Different Solvents against Some Pathogenis Microorganisms

Authors: N. Behidj, K. Benyounes, T. Dahmane, A. Allem

Abstract:

The aim of this study was to investigate the antimicrobial activity of flavonoids isolated from the aerial part of a medicinal plant which is Thymus inodorusby the middle agar diffusion method on following microorganisms. We have Staphylococcus aureus, Escherichia coli, Pseudomonas fluorescens, AspergillusNiger, Aspergillus fumigatus and Candida albicans. During this study, flavonoids extracted by stripping with steam are performed. The yields of flavonoids is 7.242% for the aqueous extract and 28.86% for butanol extract, 29.875% for the extract of ethyl acetate and 22.9% for the extract of di - ethyl. The evaluation of the antibacterial effect shows that the diameter of the zone of inhibition varies from one microorganism to another. The operation values obtained show that the bacterial strain P fluoresces, and 3 yeasts and molds; A. Niger, A. fumigatus and C. albicansare the most resistant. But it is noted that, S. aureus is shown more sensitive to crude extracts, the stock solution and the various dilutions. Finally for the minimum inhibitory concentration is estimated only with the crude extract of Thymus inodorus flavonoid.Indeed, these extracts inhibit the growth of Gram + bacteria at a concentration varying between 0.5% and 1%. While for bacteria to Gram -, it is limited to a concentration of 0.5%.

Keywords: Antimicrobial activity, flavonoids, strains, Thymus inodorus.

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40 Investigation of Anti-Inflammatory, Antipyretic and Analgesic Effect of Yemeni Sidr Honey

Authors: Aman Ahmed Alzubier, Patrick Nwabueze Okechukwu

Abstract:

Traditionally, Yemini Sidr honey has been reported to cure liver problems, stomach ulcers, and respiratory disorders. In this experiment, we evaluated Yemeni Sidr honey for its ability to protect inflammations caused by acetic acid and formalin -induced writhing, carrageenan and histamine-induced paw oedema in experimental rat model. Hyperpyrexia, membrane stabilizing activity, and phytochemical screening of the honey was also examined. Yemini Sidr Honey at (100, 200 and 500 mg/kg) exhibited a concentration dependant inhibition of acetic acid induced and formalin induced writhing, paw oedema induced by carrageenan & histamine, and hyperpyrexia induced by brewer's yeast, it also inhibited membrane stabilizing activity. Phytochemical screenings of the honey reveal the presence of flavonoids, steroid, alkaloids, saponins and tannins. This study suggested that Yemeni Sidr honey possess very strong antiinflammatory, analgesic and antipyretic effects and these effects would be a result of the phytochemicals present.

Keywords: Anti-inflammatory, Analgesic, Carrageenan, Aceticacid, Histamine, Yemini Sidr Honey

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39 Characterization and Evaluation of the Activity of Dipeptidyl Peptidase IV from the Black-Bellied Hornet Vespa basalis

Authors: Feng Chia Hsieh, Sheng Kuo Hsieh, Tzyy Rong Jinn

Abstract:

Characterization and evaluation of the activity of Vespa basalis DPP-IV, which expressed in Spodoptera frugiperda 21 cells. The expression of rDPP-IV was confirmed by SDS–PAGE, Western blot analyses, LC-MS/MS and measurement of its peptidase specificity. One-step purification by Ni-NTA affinity chromatography and the total amount of rDPP-IV recovered was approximately 6.4mg per liter from infected culture medium; an equivalent amount would be produced by 1x109 infected Sf21 insect cells. Through the affinity purification led to highly stable rDPP-IV enzyme was recovered and with significant peptidase activity. The rDPP-IV exhibited classical Michaelis–Menten kinetics, with kcat/Km in the range of 10-500 mM-1×S-1 for the five synthetic substrates and optimum substrate is Ala-Pro-pNA. As expected in inhibition assay, the enzymatic activity of rDPP-IV was significantly reduced by 80 or 60% in the presence of sitagliptin (a DPP-IV inhibitor) or PMSF (a serine protease inhibitor), but was not apparently affected by iodoacetamide (a cysteine protease inhibitor).

Keywords: Dipeptidyl-Peptidase IV, Phenylmethylsulfonyl fluoride; Serine protease, Sitagliptin, Vespa basalis

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38 Extracellular Protein Secreted by Bacillus subtilis ATCC21332 in the Presence of Streptomycin Sulfate

Authors: Hanina M. N., Hairul Shahril M., Ismatul Nurul Asyikin I., Abdul Jalil A. K., Salina M. R., Maryam M. R., Rosfarizan M.

Abstract:

The extracellular proteins secreted by bacteria may be increased in stressful surroundings, such as in the presence of antibiotics. It appears that many antibiotics, when used at low concentrations, have in common the ability to activate or repress gene transcription, which is distinct from their inhibitory effect. There have been comparatively few studies on the potential of antibiotics as a specific chemical signal that can trigger a variety of biological functions. Therefore, this study was carried out to determine the effect of Streptomycin Sulfate in regulating extracellular proteins secreted by Bacillus subtilis ATCC21332. Results of Microdilution assay showed that the Minimum Inhibition Concentration (MIC) of Streptomycin Sulfate on B. subtilis ATCC21332 was 2.5 mg/ml. The bacteria cells were then exposed to Streptomycin Sulfate at concentration of 0.01 MIC before being further incubated for 48h to 72 h. The extracellular proteins secreted were then isolated and analyzed by sodium dodecyl sulfate polyacrylamide gel electrophoresis (SDS-PAGE). Proteins profile revealed that three additional bands with approximate sizes of 30 kDa, 22 kDa and 23 kDa were appeared for the treated bacteria with Streptomycin Sulfate. Thus, B. subtilis ATCC21332 in stressful condition with the presence of Streptomycin Sulfate at low concentration could induce the extracellular proteins secretion.

Keywords: Bacillus subtilis ATCC21332, Streptomycin Sulfate, extracellular proteins.

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37 Oil Palm Empty Fruit Bunch as a New Organic Filler for Electrical Tree Inhibition

Authors: M. H. Ahmad, A. A. A. Jamil, H. Ahmad, M. A. M. Piah, A. Darus, Y. Z. Arief, N. Bashir

Abstract:

The use of synthetic retardants in polymeric insulated cables is not uncommon in the high voltage engineering to study electrical treeing phenomenon. However few studies on organic materials for the same investigation have been carried. .This paper describes the study on the effects of Oil Palm Empty Fruit Bunch (OPEFB) microfiller on the tree initiation and propagation in silicone rubber with different weight percentages (wt %) of filler to insulation bulk material. The weight percentages used were 0 wt % and 1 wt % respectively. It was found that the OPEFB retards the propagation of the electrical treeing development. For tree inception study, the addition of 1(wt %) OPEFB has increase the tree inception voltage of silicone rubber. So, OPEFB is a potential retardant to the initiation and growth of electrical treeing occurring in polymeric materials for high voltage application. However more studies on the effects of physical and electrical properties of OPEFB as a tree retardant material are required.

Keywords: Oil palm empty fruit bunch, electrical tree, siliconerubber, fillers.

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36 Comparative Studies on Interactions of Synthetic and Natural Compounds with Hen Egg-White Lysozyme

Authors: Seifollah Bahramikia

Abstract:

Amyloid aggregation of polypeptides is related to a growing number of pathologic states known as amyloid disorders. In recent years, blocking or reversing amyloid aggregation via the use of small compounds are considered as two useful approaches in hampering the development of these diseases. In this research, we have compared the ability of several manganese-salen derivatives, as synthetic compounds, and apigenin, as a natural flavonoid, to inhibit of hen egg-white lysozyme (HEWL) aggregation, as an in vitro model system. Different spectroscopic analyses such as Thioflavin T (ThT) and Anilinonaphthalene-8-sulfonic acid (ANS) fluorescence, Congo red (CR) absorbance along with transmission electron microscopy were used in this work to monitor the HEWL aggregation kinetic and inhibition. Our results demonstrated that both type of compounds were capable to prevent the formation of lysozyme amyloid aggregation in vitro. In addition, our data indicated that synthetic compounds had higher activity to inhibit of the β-sheet structures relative to natural compound. Regarding the higher antioxidant activities of the salen derivatives, it can be concluded that in addition to aromatic rings of each of the compounds, the potent antioxidant properties of salen derivatives contributes to lower lysozyme fibril accumulation.

Keywords: Aggregation, anti-amyloidogenic, apigenin, hen egg white lysozyme, salen derivatives.

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35 Discovery of Human HMG-Coa Reductase Inhibitors Using Structure-Based Pharmacophore Modeling Combined with Molecular Dynamics Simulation Methodologies

Authors: Minky Son, Chanin Park, Ayoung Baek, Shalini John, Keun Woo Lee

Abstract:

3-hydroxy-3-methylglutaryl coenzyme A reductase (HMGR) catalyzes the conversion of HMG-CoA to mevalonate using NADPH and the enzyme is involved in rate-controlling step of mevalonate. Inhibition of HMGR is considered as effective way to lower cholesterol levels so it is drug target to treat hypercholesterolemia, major risk factor of cardiovascular disease. To discover novel HMGR inhibitor, we performed structure-based pharmacophore modeling combined with molecular dynamics (MD) simulation. Four HMGR inhibitors were used for MD simulation and representative structure of each simulation were selected by clustering analysis. Four structure-based pharmacophore models were generated using the representative structure. The generated models were validated used in virtual screening to find novel scaffolds for inhibiting HMGR. The screened compounds were filtered by applying drug-like properties and used in molecular docking. Finally, four hit compounds were obtained and these complexes were refined using energy minimization. These compounds might be potential leads to design novel HMGR inhibitor.

Keywords: Anti-hypercholesterolemia drug, HMGR inhibitor, Molecular dynamics simulation, Structure-based pharmacophore modeling.

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34 The Antibacterial Efficacy of Gold Nanoparticles Derived from Gomphrena celosioides and Prunus amygdalus (Almond) Leaves on Selected Bacterial Pathogens

Authors: M. E. Abalaka, S. Y. Daniyan, S. O. Adeyemo, D. Damisa

Abstract:

Gold nanoparticles (AuNPs) have gained increasing interest in recent times. This is greatly due to their special features, which include unusual optical and electronic properties, high stability and biological compatibility, controllable morphology and size dispersion, and easy surface functionalization. In typical synthesis, AuNPs were produced by reduction of gold salt AuCl4 in an appropriate solvent. A stabilizing agent was added to prevent the particles from aggregating. The antibacterial activity of different sizes of gold nanoparticles was investigated against Staphylococcus aureus, Salmonella typhi and Pseudomonas pneumonia using the disk diffusion method in a Müeller–Hinton Agar. The Au-NPs were effective against all bacteria tested. That the Au-NPs were successfully synthesized in suspension and were used to study the antibacterial activity of the two medicinal plants against some bacterial pathogens suggests that Au-NPs can be employed as an effective bacteria inhibitor and may be an effective tool in medical field. The study clearly showed that the Au-NPs exhibiting inhibition towards the tested pathogenic bacteria in vitro could have the same effects in vivo and thus may be useful in the medical field if well researched into.

Keywords: Gold Nanoparticles, Gomphrena celesioides, Prunus amygdalus, Pathogens.

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33 Investigation on Toxicity of Manufactured Nanoparticles to Bioluminescence Bacteria Vibrio fischeri

Authors: E. Binaeian, SH. Soroushnia

Abstract:

Acute toxicity of nano SiO2, ZnO, MCM-41 (Meso pore silica), Cu, Multi Wall Carbon Nano Tube (MWCNT), Single Wall Carbon Nano Tube (SWCNT) , Fe (Coated) to bacteria Vibrio fischeri using a homemade luminometer , was evaluated. The values of the nominal effective concentrations (EC), causing 20% and 50% inhibition of biouminescence, using two mathematical models at two times of 5 and 30 minutes were calculated. Luminometer was designed with Photomultiplier (PMT) detector. Luminol chemiluminescence reaction was carried out for the calibration graph. In the linear calibration range, the correlation coefficients and coefficient of Variation (CV) were 0.988 and 3.21% respectively which demonstrate the accuracy and reproducibility of the instrument that are suitable. The important part of this research depends on how to optimize the best condition for maximum bioluminescence. The culture of Vibrio fischeri with optimal conditions in liquid media, were stirring at 120 rpm at a temperature of 150C to 180C and were incubated for 24 to 72 hours while solid medium was held at 180C and for 48 hours. Suspension of nanoparticles ZnO, after 30 min contact time to bacteria Vibrio fischeri, showed the highest toxicity while SiO2 nanoparticles showed the lowest toxicity. After 5 min exposure time, the toxicity of ZnO was the strongest and MCM-41 was the weakest toxicant component.

Keywords: Bioluminescence, effective concentration, nanomaterials, toxicity, Vibrio fischeri.

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32 Weakened Vortex Shedding from a Rotating Cylinder

Authors: Sharul S. Dol

Abstract:

An experimental study of the turbulent near wake of a rotating circular cylinder was made at a Reynolds number of 2000 for velocity ratios, λ between 0 and 2.7. Particle image velocimetry data are analyzed to study the effects of rotation on the flow structures behind the cylinder. The results indicate that the rotation of the cylinder causes significant changes in the vortex formation. Kármán vortex shedding pattern of alternating vortices gives rise to strong periodic fluctuations of a vortex street for λ < 2.0. Alternate vortex shedding is weak and close to being suppressed at λ = 2.0 resulting a distorted street with vortices of alternating sense subsequently being found on opposite sides. Only part of the circulation is shed due to the interference in the separation point, mixing in the base region, re-attachment, and vortex cut-off phenomenon. Alternating vortex shedding pattern diminishes and completely disappears when the velocity ratio is 2.7. The shed vortices are insignificant in size and forming a single line of vortex street. It is clear that flow asymmetries will deteriorate vortex shedding, and when the asymmetries are large enough, total inhibition of a periodic street occurs.

Keywords: Circulation, particle image velocimetry, rotating circular cylinder, smoke-wire flow visualization, Strouhal number, vortex shedding, vortex street.

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31 Computer Aided Drug Design and Studies of Antiviral Drug against H3N2 Influenza Virus

Authors: Aditi Shukla, Ambarish S. Vidyarthi, Subir Samanta

Abstract:

The worldwide prevalence of H3N2 influenza virus and its increasing resistance to the existing drugs necessitates for the development of an improved/better targeting anti-influenza drug. H3N2 influenza neuraminidase is one of the two membrane-bound proteins belonging to group-2 neuraminidases. It acts as key player involved in viral pathogenicity and hence, is an important target of anti-influenza drugs. Oseltamivir is one of the potent drugs targeting this neuraminidase. In the present work, we have taken subtype N2 neuraminidase as the receptor and probable analogs of oseltamivir as drug molecules to study the protein-drug interaction in anticipation of finding efficient modified candidate compound. Oseltamivir analogs were made by modifying the functional groups using Marvin Sketch software and were docked using Schrodinger-s Glide. Oseltamivir analog 10 was detected to have significant energy value (16% less compared to Oseltamivir) and could be the probable lead molecule. It infers that some of the modified compounds can interact in a novel manner with increased hydrogen bonding at the active site of neuraminidase and it might be better than the original drug. Further work can be carried out such as enzymatic inhibition studies; synthesis and crystallizing the drug-target complex to analyze the interactions biologically.

Keywords: H3N2 Influenza, Neuraminidase, Oseltamiviranalogs, structure based drug designing

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30 The Correlation of Total Phenol Content with Free Radicals Scavenging Activity and Effect of Ethanol Concentration in Extraction Process of Mangosteen Rind (Garcinia mangostana)

Authors: Ririn Lestari Sri Rahayu, Mustofa Ahda

Abstract:

The use of synthetic antioxidants often causes a negative effect on health and increases the incidence of carcinogenesis. Development of the natural antioxidants should be investigated. However, natural antioxidants have a low toxicity and are safe for human consumption. Ethanol extract of mangosteen rind (Garcinia mangostana) contains natural antioxidant compounds that have various pharmacological activities. Antioxidants from the ethanol extract of mangosteen rind have free radicals scavenging activities. The scavenging activity of ethanol extract of mangosteen rind was determined by DPPH method. The phenolic compound from the ethanol extract of mangosteen rind is determined with Folin-Ciocalteu method. The results showed that the absolute ethanol extract of mangosteen rind has IC50 of 40.072 ug/mL. The correlation of total phenols content with free radical scavenging activity has an equation y: 5.207x + 205.51 and determination value (R2) of 0.9329. Total phenols content from the ethanol extract of mangosteen rind has a good correlation with free radicals scavenging activity of DPPH.

Keywords: Antioxidant, Garcinia mangostana, inhibition concentration 50%, total phenolic compounds.

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29 Study of Functional Relevant Conformational Mobility of β-2 Adrenoreceptor by Means of Molecular Dynamics Simulation

Authors: G. V. Novikov, V. S. Sivozhelezov, S. S. Kolesnikov, K. V. Shaitan

Abstract:

The study reports about the influence of binding of orthosteric ligands as well as point mutations on the conformational dynamics of β-2-adrenoreceptor. Using molecular dynamics simulation we found that there was a little fraction of active states of the receptor in its apo (ligand free) ensemble corresponded to its constitutive activity. Analysis of MD trajectories indicated that such spontaneous activation of the receptor is accompanied by the motion in intracellular part of its alpha-helices. Thus receptor’s constitutive activity directly results from its conformational dynamics. On the other hand the binding of a full agonist resulted in a significant shift of the initial equilibrium towards its active state. Finally, the binding of the inverse agonist stabilized the receptor in its inactive state. It is likely that the binding of inverse agonists might be a universal way of constitutive activity inhibition in vivo. Our results indicate that ligand binding redistribute pre-existing conformational degrees of freedom (in accordance to the Monod-Wyman-Changeux-Model) of the receptor rather than cause induced fit in it. Therefore, the ensemble of biologically relevant receptor conformations is encoded in its spatial structure, and individual conformations from that ensemble might be used by the cell in conformity with the physiological behavior.

Keywords: Seven-transmembrane receptors, constitutive activity, activation, x-ray crystallography, principal component analysis, molecular dynamics simulation.

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28 Protein Production by Bacillus Subtilis Atcc 21332 in the Presence of Cymbopogon Essential Oils

Authors: Hanina M. N., Hairul Shahril M., Mohd Fazrullah Innsan M. F., Ismatul Nurul Asyikin I., Abdul Jalil A. K, Salina M. R., Ahmad I.B.

Abstract:

Proteins levels produced by bacteria may be increased in stressful surroundings, such as in the presence of antibiotics. It appears that many antimicrobial agents or antibiotics, when used at low concentrations, have in common the ability to activate or repress gene transcription, which is distinct from their inhibitory effect. There have been comparatively few studies on the potential of antibiotics or natural compounds in nature as a specific chemical signal that can trigger a variety of biological functions. Therefore, this study was focusing on the effect of essential oils from Cymbopogon flexuosus and C. nardus in regulating proteins production by Bacillus subtilis ATCC 21332. The Minimum Inhibition Concentrations (MICs) of both essential oils on B. subtilis were determined by using microdilution assay, resulting 0.2% and 1.56% for each C. flexuosus and C. nardus subsequently. The bacteria were further exposed to each essential oils at concentration of 0.01XMIC for 2 days. The proteins were then isolated and analyzed by sodium dodecyl sulfate polyacrylamide gel electrophoresis (SDS-PAGE). Protein profile showed that a band with approximate size of 250 kD was appeared for the treated bacteria with essential oils. Thus, Bacillus subtilis ATCC 21332 in stressful condition with the presence of essential oils at low concentration could induce the protein production.

Keywords: Bacillus subtilis ATCC 21332, Cymbopogon essential oils, protein

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27 Hypoglycemic Activity of Water Soluble Polysaccharides of Yam (Dioscorea hispida Dents) Prepared by Aqueous, Papain, and Tempeh Inoculum Assisted Extractions

Authors: Teti Estiasih, Harijono, Weny Bekti Sunarharum, Atina Rahmawati

Abstract:

This research studied the hypoglycemic effect of water soluble polysaccharide (WSP) extracted from yam (Dioscorea hispida) tuber by three different methods: aqueous extraction, papain assisted extraction, and tempeh inoculums assisted extraction. The two later extraction methods were aimed to remove WSP binding protein to have more pure WSP. The hypoglycemic activities were evaluated by means in vivo test on alloxan induced hyperglycemic rats, glucose response test (GRT), in situ glucose absorption test using everted sac, and short chain fatty acids (SCFAs) analysis. All yam WSP extracts exhibited ability to decrease blood glucose level in hyperglycemia condition as well as inhibited glucose absorption and SCFA formation. The order of hypoglycemic activity was tempeh inoculums assisted- >papain assisted- >aqueous WSP extracts. GRT and in situ glucose absorption test showed that order of inhibition was papain assisted- >tempeh inoculums assisted- >aqueous WSP extracts. Digesta of caecum of yam WSP extracts oral fed rats had more SCFA than control. Tempeh inoculums assisted WSP extract exhibited the most significant hypoglycemic activity.

Keywords: hypoglycemic activity, papain, tempeh inoculums, water soluble polysaccharides, yam (Discorea hispida)

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26 Laxative Potential of The Konjac Flour (Amorphophallus muelleri Blume) in Treatment of Loperamide Induced Constipation on Sprague Dawley Rats

Authors: Simon Bambang Widjanarko, Novita Wijayanti, Aji Sutrisno

Abstract:

There is long history of konjac tubers being used as a cure for certain diseases in China and Japan. Konjac flour is prepared from konjac tubers and it contains high concentration of glucomannan. Konjac Glucomannan (KGM) is dietary fiber and the role of which has been demonstrated in weight reduction, lowering blood cholesterol and sugar level, promoting intestinal activity etc. Konjac glucomanan has a property of swelling by absorbing water, more than a hundred times its own weight. Therefore it helps increasing weight of feces, water content of feces, and promotes satiety feeling. Mode of actions of dietary fibre as laxatives agents includes holding water inside the bowel lumen, inhibition of water absorption in the colon and stimulating colonic motility. Number of fecal pellets did not effected in rats were fed on 300 and 600 mg/kg of konjac flour, as well as constipated control and Dulcolax treatment. Water content, weight of fecal pellets and gastrointestinal transit ratio were higher in rats treated with 600 mg/kg than 300 mg/kg of konjac flour. Rats were administered with Dulcolax showed the highest gastrointestinal transit ratio, followed by 600 mg/kg konjac flour. The lowest feed consumption was noted in 600 mg/kg konjac flour diet group.

Keywords: Laxative, konjac flour, Amorphophallus muelleri Blume, glucomannan, constipation.

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25 The Effects of Soil Parameters on Efficiency of Essential Oil from Zingiber zerumbet (L.) Smith in Thailand

Authors: Worakrit Worananthakij, Kamonchanok Doungtadum, Nattagan Mingkwan, Supatsorn Chupong

Abstract:

Natural products from herb have been used in different aspects of life as a result of their various biological activities. Generally, plant growth and production of secondary compounds largely depend on environmental conditions. To better understand this correlation, study on biological activity and soil parameter is necessary. This research aims to study the soil parameters which affect the efficiency of the antioxidant activity of essential oils extracted from the Zingiber zerumbet in three areas of Thailand, including Min Buri district, Bangkok province; Muang district, Chiang Mai province and Kaeng Sanam Nang district, Nakhon Ratchasima province. The soil samples in each area were collected and analyzed in the laboratory. The essential oil of Z. zerumbet in each province was extracted and tested for antioxidant activity by hydrodistillation method and DPPH (2,2-diphenyl-1-picrylhydrazyl radical) assay, respectively. The results showed that, the soil parameters such as pH, nitrogen, potassium and phosphorus elements and exchange of cations of soil specimen from Nakhon Ratchasima province were the highest (P<0.05) (6.10 ±0.03, 0.15 ± 0.04 percent of total nitrogen, 16.67 ± 0.46 mg/L, 3.35 ± 0.65 mg/kg and 12.87 ± 0.11 cmol/kg, respectively). In addition, IC50 (Inhibition Concentrtion of antioxidant at 50%) of Z. zerumbet essential oil collected from Nakhon Ratchasima showed the highest value (P<0.05) (1,400 µg/mL). In conclusion, the soil parameters are once important factor for the efficiency of essential oils extract from Z. zerumbet.

Keywords: Antioxidant, essential oil, herb, soil parameter, Zingiber zerumbet.

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24 Hydropriming and Osmopriming Effects on Cumin(Cuminum Cyminum L.) Seeds Germination

Authors: E. Neamatollahi, M. Bannayan, A. Souhani Darban, A. Ghanbari

Abstract:

In production of medicinal plants, seed germination is very important problem. The treated seeds (control, hydro priming and ZnSO4) of Cumin (Cuminum cyminum L.) were evaluated at germination and seedling growth for tolerance to salt (NaCl and Na2SO4) conditions at the same water potentials of 0.0, -0.3, -0.6, - 0.9 and -1.2MPa. Electrical conductivity (EC) values of the NaCl solutions were 0.0, 6.5, 12.7, 18.4 and 23.5 dSm-1, respectively. The objective of the study was to determine factors responsible for germination and early seedling growth due to salt toxicity or osmotic effect and to optimize the best priming treatment for these stress conditions. Results revealed that germination delayed in both solutions, having variable germination with different priming treatments. Germination, shoot and weight, root and shoot length were higher but mean germination time and abnormal germination percentage were lower in NaCl than Na2SO4 at the same water potential. The root / shoot weight and R/S length increased with increase in osmotic potential in both NaCl and Na2SO4 solutions. NaCl had less inhibitor effect on seedling growth than the germination. It was concluded that inhibition of germination at the same water potential of NaCl and Na2SO4 resulted from salt toxicity rather than osmotic effect. Hydro priming increased germination and seedling growth under salt stress. This protocol has practical importance and could be recommended to farmers to achieve higher germination and uniform emergence under field conditions.

Keywords: Priming, Germination, Nacl, ZnSo4, Na2So4.

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23 The Use of Palm Kernel Shell and Ash for Concrete Production

Authors: J. E. Oti, J. M. Kinuthia, R. Robinson, P. Davies

Abstract:

This work reports the potential of using Palm Kernel (PK) ash and shell as a partial substitute for Portland Cement (PC) and coarse aggregate in the development of mortar and concrete. PK ash and shell are agro-waste materials from palm oil mills, the disposal of PK ash and shell is an environmental problem of concern. The PK ash has pozzolanic properties that enables it as a partial replacement for cement and also plays an important role in the strength and durability of concrete, its use in concrete will alleviate the increasing challenges of scarcity and high cost of cement. In order to investigate the PC replacement potential of PK ash, three types of PK ash were produced at varying temperature (350-750C) and they were used to replace up to 50% PC. The PK shell was used to replace up to 100% coarse aggregate in order to study its aggregate replacement potential. The testing programme included material characterisation, the determination of compressive strength, tensile splitting strength and chemical durability in aggressive sulfatebearing exposure conditions. The 90 day compressive results showed a significant strength gain (up to 26.2 N/mm2). The Portland cement and conventional coarse aggregate has significantly higher influence in the strength gain compared to the equivalent PK ash and PK shell. The chemical durability results demonstrated that after a prolonged period of exposure, significant strength losses in all the concretes were observed. This phenomenon is explained, due to lower change in concrete morphology and inhibition of reaction species and the final disruption of the aggregate cement paste matrix.

Keywords: Sustainability, Concrete, mortar, Palm kernel shell, compressive strength, consistency.

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22 Differential Sensitivity of Nitrogen-Fixing, Filamentous Cyanobacterial Species to an Organochlorine Insecticide - 6, 7, 8, 9, 10, 10- Hexachloro-1, 5, 5a, 6, 9, 9a-Hexahydro-6, 9- Methano-2, 4, 3-Benzodioxathiepine-3-Oxide

Authors: Nirmal J.I. Kumar, Anubhuti A. Bora, Manmeet K. Amb

Abstract:

Application of pesticides in the paddy fields has deleterious effects on non-target organisms including cyanobacteria which are photosynthesizing and nitrogen fixing micro-organisms contributing significantly towards soil fertility and crop yield. Pesticide contamination in the paddy fields has manifested into a serious global environmental concern. To study the effect of one such pesticide, three cyanobacterial strains; Anabaena fertilissima, Aulosira fertilissima and Westiellopsis prolifica were selected for their stress responses to an Organochlorine insecticide - 6, 7, 8, 9, 10, 10-hexachloro-1, 5, 5a, 6, 9, 9a-hexahydro-6, 9-methano-2, 4, 3- benzodioxathiepine-3-oxide, with reference to their photosynthesic pigments-chlorophyll-a and carotenoids as well as accessory pigments-phycobiliproteins (phycocyanin, allophycocyanin and phycoerythrin), stress induced biochemical metabolites like carbohydrates, proteins, amino acids, phenols and enzymes-nitrate reductase, glutamine synthetase and succinate dehydrogenase. All the three cyanobacterial strains were adversely affected by the insecticide doses and inhibition was dose dependent. Reduction in photosynthetic and accessory pigments, metabolites, nitrogen fixing and respiratory enzymes of the test organisms were accompanied with an initial increase in their total protein at lower Organochlorine doses. On the other hand, increased amount of phenols in all the insecticide treated concentrations was indicative of stressed activities of the organisms.

Keywords: biochemical metabolites, endosulfan, enzymes, pigments

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21 Ellagic Acid Enhanced Apoptotic Radiosensitivity via G1 Cell Cycle Arrest and γ-H2AX Foci Formation in HeLa Cells in vitro

Authors: V. R. Ahire, A. Kumar, B. N. Pandey, K. P. Mishra, G. R. Kulkarni

Abstract:

Radiation therapy is an effective vital strategy used globally in the treatment of cervical cancer. However, radiation efficacy principally depends on the radiosensitivity of the tumor, and not all patient exhibit significant response to irradiation. A radiosensitive tumor is easier to cure than a radioresistant tumor which later advances to local recurrence and metastasis. Herbal polyphenols are gaining attention for exhibiting radiosensitization through various signaling. Current work focuses to study the radiosensitization effect of ellagic acid (EA), on HeLa cells. EA intermediated radiosensitization of HeLa cells was due to the induction γ-H2AX foci formation, G1 phase cell cycle arrest, and loss of reproductive potential, growth inhibition, drop in the mitochondrial membrane potential and protein expression studies that eventually induced apoptosis. Irradiation of HeLa in presence of EA (10 μM) to doses of 2 and 4 Gy γ-radiation produced marked tumor cytotoxicity. EA also demonstrated radio-protective effect on normal cell, NIH3T3 and aided recovery from the radiation damage. Our results advocate EA to be an effective adjuvant for improving cancer radiotherapy as it displays striking tumor cytotoxicity and reduced normal cell damage instigated by irradiation.

Keywords: Apoptotic radiosensitivity, ellagic acid, mitochondrial potential, cell-cycle arrest.

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