Search results for: selective inhibition of Cdk5/p25

Authors: P. Gayathri, G. P. Jeyanthi

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The bark of Polyalthia longifolia is used in ayurvedic system of medicine for the manangement of various ailments including diabetes mellitus. The bark of P. longifolia extracts was extracted using various polar and non-polar solvents and tested for inhibition of alpha-amylase and alpha-glucosidase among which the ethanolic extracts were found to be more potent. The ethanolic extracts of the bark were tested for the in vitro inhibition of alpha-amylase using starch as substrate and alpha-glucosidase using p-nitro phenyl alpha-D-gluco pyranoside as substrate to establish its in vitro antidiabetic effect. The mechanism of inhibition was determined by Dixon plot and Cornish-Bowden plot. The cytotoxic effect of the extract was tested on L6 and Vero cell-lines. The extract was partially purified by TLC. The individual effect of the ethanolic extract, TLC fractions and its combinatorial effect with insulin and glibenclamide on glucose uptake by rat hemi-diaphragm were studied.Results revealed that the ethanolic extracts of Polyalthia longifolia bark exhibited competitive inhibition of alpha-amylase and alpha-glucosidase. The extracts were also found not to be cytotoxic at the highest dose of 1 mg/mL. Glucose uptake study revealed that the extract alone and when combined with insulin, decreased the glucose uptake when compared to insulin control, however the purified TLC fractions exhibited significantly higher (p<0.05) glucose uptake by the rat hemi-diaphragm when compared to insulin. The study shows various possible mechanism of in vitro antidiabetic effect of the P. longifolia bark.

Keywords: alpha-amylase, alpha-glucosidase, dixon, cornish-bowden, L6 , Vero cell-lines, glucose uptake, polyalthia longifolia bark, ethanolic extract, TLC fractions

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Authors: Fang-Bo Yu, Li-Bo Guan, Sheng-Dao Shan

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Biogas slurry was mixed with six commercial fungicides and screening against 11 phytopathogens was carried out. Results showed that inhibition of biogas slurry was different for the test strains and no significant difference between treatments of Didymella bryoniae, Fusarium oxysporum f. sp. vasinfectum, Aspergillus niger, Rhizoctonia cerealis, F. graminearum and Septoria tritici was observed. However, significant differences were found among Penicillium sp., Botrytis cinerea, Alternaria sonali, F. oxysporum F. sp. melonis and Sclerotinia sclerotiorum. The approach described here presents a promising alternative to current manipulation although some issues still need further examination. This study could contribute to the development of sustainable agriculture and better utilization of biogas slurry.

Keywords: anaerobic digestion, biogas slurry, phytopathogen, sustainable agriculture

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Authors: Devasis Ghosh

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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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Authors: Parinaz Tavakoli Zaniani, Dimitrios Balomenos

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Mitochondrial reactive oxygen species (mROS) play a crucial role in macrophage pro-inflammatory activation, although a detailed understanding of the mechanism and kinetics by which mROS drive signaling molecules is still lacking. In general, it is thought that NF-κB activation drives mROS and general ROS production. Here, We performed a detailed kinetic analysis of mROS production during macrophage activation. We found early mROS generation after LPS (lipopolysaccharide) stimulation. Remarkably as early as 5 minutes, mROS signaling promoted initial NF-κB, MAPK activation and pro-inflammatory cytokine production, as established through inhibition or quenching of mROS. On the contrary, NF-κB inhibition had no effect on mROS production. Our findings point to a mechanism by which mROS increase TRAF-6 ubiquitination and, thus NF-κB activity. mROS inhibition reduced LPS-induced lethality in an in vivo septic shock model by controlling pro-inflammatory cytokine production. Overall, our research provides novel insights into the role of mROS as a primary messenger in the pathway of macrophage and as a regulator of inflammatory responses. We found that early mROS production promotes initial NF-κB, and MAPK activation by regulating TRAF-6 ubiquitination and that mROS inhibition can reduce LPS-induced inflammatory cytokines and lethality in a septic shock model. These findings might lead to novel immunotherapeutic strategies targeting early mROS production and control of extreme inflammation in the context of sepsis and other inflammatory diseases.

Keywords: mitochondria, reactive oxygen species, nuclear factor κB, lipopolysaccharide, macrophages

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Authors: Priyanka Chowdhury, Asitikantha Sarma, Utpal Ghosh

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Hadron therapy using high Linear Energy Transfer (LET) ion beam is producing promising clinical results worldwide. The major advantages are its ability to kill radio-resistant tumor and its anti-metastatic activity. Poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors have been widely used as radiosensitizer, but its role in metastasis is unknown. The purpose of our study was to investigate the effect of PARP-1 depletion in combination with either Carbon Ion Beam (CIB) or gamma irradiation on metastatic potential of cultured cancerous cells. A549 cells were irradiated with CIB (0-4Gy) or gamma (0, 2, 4, 6 and 10 Gy) with and without PARP-1 inhibition. The metastatic potential of the cells was determined by cell migratory assay, expression, and activity of MMP-2 and MMP-9, expression of Cadherin, Fibronectin, and Vimentin. CIB exposure reduced migratory property and activity of MMP-2 and MMP-9 significantly. CIB with PARP-1 inhibition reduced cell migration and Matrix Metalloproteinase (MMPs) activity in a synergistic manner. Expression of MMPs was also down-regulated in CIB and combined treatment. On the contrary, MMP- 2 and MMP-9 activity was significantly increased in gamma irradiated cells but decreased upon combined treatment of gamma and PARP-1 inhibitor. MMPs expression and migration was reduced when gamma irradiation was combined with PARP-1 inhibition. Thus, our study clearly demonstrates that PARP-1 inhibition in combination with either high or low LET can significantly suppress metastatic potential in cancer cells and thereby can be a promising tool in controlling metastatic cancers.

Keywords: high LET, low LET, matrix metalloproteinase (MMP), PARP-1

Procedia PDF Downloads 192

Authors: Kiran Nawaz, Waheed Anwar, Sehrish Iftikhar, Muhammad Nasir Subhani, Ahmad Ali Shahid

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Plant growth promoting rhizobacteria (PGPR) have been extensively studied and applied for the biocontrol of many soilborne diseases. These rhizobacteria are very efficient against root rot and many other foliar diseases associated with solanaceous plants. These bacteria may inhibit the growth of various pathogens through direct inhibition of target pathogens or indirectly by the initiation of systemic resistance (ISR) which is active all over the complete plant. In the present study, 20 different rhizobacterial isolates were recovered from the root zone of healthy chili plants. All soil samples were collected from various chili-growing areas in Punjab. All isolated rhizobacteria species were evaluated in vitro and in vivo against Phytophthora capsici. Different species of Bacillus and Pseudomonas were tested for the antifungal activity against P. capsici the causal organism of Root rot disease in different crops together with chili. Dual culture and distance culture bioassay were carried out to study the antifungal potential of volatile and diffusible metabolites secreted from rhizobacteria. After seven days of incubation at 22°C, growth inhibition rate was recorded. Growth inhibition rate depended greatly on the tested bacteria and screening methods used. For diffusible metabolites, inhibition rate was 35-62% and 20-45% for volatile metabolites. The screening assay for plant growth promoting and disease inhibition potential of chili associated PGPR indicated 42-100% reduction in disease severity and considerable enhancement in roots fresh weight by 55-87%, aerial parts fresh weight by 35-65% and plant height by 65-76% as compared to untreated control and pathogen-inoculated plants. Pseudomonas flourescene, B. thuringiensis, and B. subtilis were found to be the most efficient isolates in inhibiting P. capsici radial growth, increase plant growth and suppress disease severity.

Keywords: rhizobacteria, chili, phytophthora, root rot

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Authors: Zohreh Bayat, Dariush Minai-Tehrani

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

Keywords: bacteria, inhibition, kinetics, lipase

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Authors: Dipranjan Laha, Parimal Karmakar

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Metal oxide nanoparticles are well known to generate oxidative stress and deregulate normal cellular activities. Among these, transition metals copper oxide nanoparticles (CuO NPs) are more compelling than others and able to modulate different cellular responses. In this work, we have synthesized and characterized CuO NPs by various biophysical methods. These CuO NPs (~30 nm) induce autophagy in human breast cancer cell line, MCF7 in a time and dose-dependent manner. Cellular autophagy was tested by MDC staining, induction of green fluorescent protein light chain 3 (GFP-LC3B) foci by confocal microscopy, transfection of pBABE-puro mCherry-EGFP-LC3B plasmid and western blotting of autophagy marker proteins LC3B, beclin1, and ATG5. Further, inhibition of autophagy by 3-Methyladenine (3-MA) decreased LD50 doses of CuO NPs. Such cell death was associated with the induction of apoptosis as revealed by FACS analysis, cleavage of PARP, dephosphorylation of Bad and increased cleavage product of caspase3. siRNA-mediated inhibition of autophagy-related gene beclin1 also demonstrated similar results. Finally, induction of apoptosis by 3-MA in CuO NPs treated cells were observed by TEM. This study indicates that CuO NPs are a potent inducer of autophagy which may be a cellular defense against the CuO NPs mediated toxicity and inhibition of autophagy switches the cellular response into apoptosis. A combination of CuO NPs with the autophagy inhibitor is essential to induce apoptosis in breast cancer cells. Acknowledgments: The authors would like to acknowledge for financial support for this research work to the Department of Biotechnology (No. BT/PR14661/NNT/28/494/2010), Government of India.

Keywords: nanoparticle, autophagy, apoptosis, siRNA-mediated inhibition

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Authors: Christy Rosaline, Rathankar Roa, Waheeta Hopper

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Persistence of tuberculosis, emergence of multidrug-resistance and extensively drug-resistant forms of the disease, has increased the interest in developing new antitubercular drugs. Developing inhibitors for 3-deoxy-D-arabino-heptulosonate 7-phosphate synthase from Mycobacterium tuberculosis (MtbDAH7Ps), an enzyme involved in shikimate pathway, gives a selective target for antitubercular agents. MtbDAH7Ps was screened against ZINC database, and shortlisted compounds were subjected to induce fit docking. Prime/Molecular Mechanics Generalized Born Surface Area calculation was used to validate the binding energy of ligand-protein complex. Molecular Dynamics analysis for of the lead compounds–MtbDAH7Ps complexes showed that the backbone of MtbDAH7Ps in their complexes were stable. These results suggest that the shortlisted lead compounds ZINC04097114, ZINC15163225, ZINC16857013, ZINC06275603, and ZINC05331260 could be developed into novel drug leads to inhibit DAH7Ps in Mycobacterium tuberculosis.

Keywords: MtbDAH7Ps, Mycobacterium tuberculosis, HTVS, molecular dynamics

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Authors: F. Boukli Hacene, W. Soufi, S. Ghalem

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Glaucoma disease is a progressive degenerative optic neuropathy, with irreversible visual field deficits and high eye pressure being one of the risk factors. Sulfonamides are carbonic anhydrase-II inhibitors that aim to decrease the secretion of aqueous humor by direct inhibition of this enzyme at the level of the ciliary processes. These drugs present undesirable effects that are difficult to accept by the patient. In our study, we are interested in the inhibition of carbonic anhydrase-II by different natural ligands (curcumin analogues) using molecular modeling methods using molecular operating environment (MOE) software to predict their interaction with this enzyme.

Keywords: carbonic anhydrase-II, curcumin analogues, drug research, molecular modeling

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Authors: A. Newman-Tancredi, R. Depoortère, P. Gruca, E. Litwa, M. Lason, M. Papp

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The N-methyl-D-aspartic acid (NMDA) receptor antagonist, ketamine, can elicit rapid-acting antidepressant (RAAD) effects in treatment-resistant patients, but it requires parenteral co-administration with a classical antidepressant under medical supervision. In addition, ketamine can also produce serious side effects that limit its long-term use, and there is much interest in identifying RAADs based on ketamine’s mechanism of action but with safer profiles. Ketamine elicits GABAergic interneuron inhibition, glutamatergic neuron stimulation, and, notably, activation of serotonin 5-HT1A receptors in the prefrontal cortex (PFC). Direct activation of the latter receptor subpopulation with selective ‘biased agonists’ may therefore be a promising strategy to identify novel RAADs and, consistent with this hypothesis, the prototypical cortical biased agonist, NLX-101, exhibited robust RAAD-like activity in the chronic mild stress model of depression (CMS). The present study compared the effects of a novel, selective 5-HT1A receptor-biased agonist, NLX-204, with those of ketamine and NLX-101. Materials and methods: CMS procedure was conducted on Wistar rats; drugs were administered either intraperitoneally (i.p.) or by bilateral intracortical microinjection. Ketamine: 10 mg/kg i.p. or 10 µg/side in PFC; NLX-204 and NLX-101: 0.08 and 0.16 mg/kg i.p. or 16 µg/side in PFC. In addition, interaction studies were carried out with systemic NLX-204 or NLX-101 (each at 0.16 mg/kg i.p.) in combination with intracortical WAY-100635 (selective 5-HT1A receptor antagonist; 2 µg/side) or muscimol (GABA-A receptor agonist, 12.5 ng/side). Anhedonia was assessed by CMS-induced decrease in sucrose solution consumption; anxiety-like behavior was assessed using the Elevated Plus Maze (EPM), and cognitive impairment was assessed by the Novel Object Recognition (NOR) test. Results: A single administration of NLX-204 was sufficient to reverse the CMS-induced deficit in sucrose consumption, similarly to ketamine and NLX-101. NLX-204 also reduced CMS-induced anxiety in the EPM and abolished CMS-induced NOR deficits. These effects were maintained (EPM and NOR) or enhanced (sucrose consumption) over a subsequent 2-week period of treatment. The anti-anhedonic response of the drugs was also maintained for several weeks Following treatment discontinuation, suggesting that they had sustained effects on neuronal networks. A single PFC administration of NLX-204 reversed deficient sucrose consumption, similarly to ketamine and NLX-101. Moreover, the anti-anhedonic activities of systemic NLX-204 and NLX 101 were abolished by coadministration with intracortical WAY-100635 or muscimol. Conclusions: (i) The antidepressant-like activity of NLX-204 in the rat CMS model was as rapid as that of ketamine or NLX-101, supporting targeting cortical 5-HT1A receptors with selective, biased agonists to achieve RAAD effects. (ii)The anti-anhedonic activity of systemic NLX-204 was mimicked by local administration of the compound in the PFC, confirming the involvement of cortical circuits in its RAAD-like effects. (iii) Notably, the effects of systemic NLX-204 and NLX-101 were abolished by PFC administration of muscimol, indicating that they act by (indirectly) eliciting a reduction in cortical GABAergic neurotransmission. This is consistent with ketamine’s mechanism of action and suggests that there are converging NMDA and 5-HT1A receptor signaling cascades in PFC underlying the RAAD-like activities of ketamine and NLX-204. Acknowledgements: The study was financially supported by NCN grant no. 2019/35/B/NZ7/00787.

Keywords: depression, ketamine, serotonin, 5-HT1A receptor, chronic mild stress

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Authors: Nabila Mohamed, Santiago Aparicio, Bahman Tohidi, Mert Atilhan

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Qatar's one of the biggest problem in processing its natural resource, which is natural gas, is the often occurring blockage in the pipelines caused due to uncontrolled gas hydrate formation in the pipelines. Several millions of dollars are being spent at the process site to dehydrate the blockage safely by using chemical inhibitors. We aim to establish national database, which addresses the physical conditions that promotes Qatari natural gas to form gas hydrates in the pipelines. Moreover, we aim to design and test novel hydrate inhibitors that are suitable for Qatari natural gas and its processing facilities. From these perspectives we are aiming to provide more effective and sustainable reservoir utilization and processing of Qatari natural gas. In this work, we present the initial findings of a QNRF funded project, which deals with the natural gas hydrate formation characteristics of Qatari type gas in both experimental (PVTx) and computational (molecular simulations) methods. We present the data from the two fully automated apparatus: a gas hydrate autoclave and a rocking cell. Hydrate equilibrium curves including growth/dissociation conditions for multi-component systems for several gas mixtures that represent Qatari type natural gas with and without the presence of well known kinetic and thermodynamic hydrate inhibitors. Ionic liquids were designed and used for testing their inhibition performance and their DFT and molecular modeling simulation results were also obtained and compared with the experimental results. Results showed significant performance of ionic liquids with up to 0.5 % in volume with up to 2 to 4 0C inhibition at high pressures.

Keywords: gas hydrates, natural gas, ionic liquids, inhibition, thermodynamic inhibitors, kinetic inhibitors

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Authors: Jaroslaw Mizera, Pawel Wisniewski, Ryszard Sitek

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Selective Laser Melting (SLM) is an advanced additive manufacturing technique used for producing parts made of wide range of materials such as: austenitic steel, titanium, nickel etc. In the our experiment we produced a Ti-AlN composite from a mixture of titanium and aluminum nitride respectively 70% at. and 30% at. using SLM technique. In order to define the size of powder particles, laser diffraction tests were performed on HORIBA LA-950 device. The microstructure and chemical composition of the composite was examined by Scanning Electron Microscopy (SEM). The chemical composition in micro areas of the obtained samples was determined by of EDS. The phase composition was analyzed by X-ray phase analysis (XRD). Microhardness Vickers tests were performed using Zwick/Roell microhardness machine under the load of 0.2kG (HV0.2). Hardness measurements were made along the building (xy) and along the plane of the lateral side of the cuboid (xz). The powder used for manufacturing of the samples had a mean particle size of 41μm. It was homogenous with a spherical shape. The specimens were built chiefly from Ti, TiN and AlN. The dendritic microstructure was porous and fine-grained. Some of the aluminum nitride remained unmelted but no porosity was observed in the interface. The formed material was characterized by high hardness exceeding 700 HV0.2 over the entire cross-section.

Keywords: Selective Laser Melting, Composite, SEM, microhardness

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Authors: M. A. Deyab

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The effect of zwitterionic surfactant (ZS) on erosion-corrosion of API X52 steel in oil sands slurry was studied using Tafel polarization and anodic polarization measurements. The surface morphology of API X52 steel was examined with scanning electron microscopy (SEM) and atomic force microscopy (AFM). ZS inhibited the erosion-corrosion of API X52 steel in oil sands' slurry, and the inhibition efficiency increased with increasing ZS concentration but decreased with increasing temperature. Polarization curves indicate that ZS act as a mixed type of inhibitor. Inhibition efficiencies of ZS in the dynamic condition are not as effective as that obtained in the static condition.

Keywords: corrosion, surfactant, oil sands slurry, erosion-corrosion

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Authors: Ibrahim Mostafa El-Mongy, Abdelmegid Allam

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In this article analysis and investigation of the effect of loading a horn antenna with substrate integrated waveguide frequency selective surface (SIW FSS) of crossed dipoles of finite size is presented. It is fabricated on Rogers RO4350 (lossy) of relative permittivity 3.33, thickness 1.524mm and loss tangent 0.004. This structure is called a filtering antenna (filtenna). Basically it is applied for filtering and minimizing the interference and noise in the desired band. The filtration is carried out using a finite SIW FSS of crossed dipoles of overall dimensions 98x58 mm2. The filtration is shown by limiting the transmission bandwidth from 4 GHz (8–12 GHz) to 0.3 GHz (0.955–0.985 GHz). It is simulated using CST MWS and measured using network analyzer. There is a good agreement between the simulated and measured results.

Keywords: antenna, filtenna, frequency-selective surface (FSS), horn antennas

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Authors: Amarpreet Singh, Kimi Manchanda

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Intended for providing the security in the VANETS (Vehicular Ad hoc Network) scenario, the covert storage channel is implemented through data transmitted between the sender and the receiver. Covert channels are the logical links which are used for the communication purpose and hiding the secure data from the intruders. This paper refers to the Establishment of bit selective mode covert storage channels in VANETS. In this scenario, the data is being transmitted with two modes i.e. the normal mode and the covert mode. During the communication between vehicles in this scenario, the controlling of bits is possible through the optional bits of IPV6 Header Format. This implementation is fulfilled with the help of Network simulator.

Keywords: covert mode, normal mode, VANET, OBU, on-board unit

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Authors: P. Krachodnok

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In this paper, the design of a multiple U-slotted microstrip patch antenna with frequency selective surface (FSS) as a superstrate for WLAN and WiMAX applications is presented. The proposed antenna is designed by using substrate FR4 having permittivity of 4.4 and air substrate. The characteristics of the antenna are designed and evaluated the performance of modelled antenna using CST Microwave studio. The proposed antenna dual resonant frequency has been achieved in the band of 2.37-2.55 GHz and 3.4-3.6 GHz. Because of the impact of FSS superstrate, it is found that the bandwidths have been improved from 6.12% to 7.35 % and 3.7% to 5.7% at resonant frequencies 2.45 GHz and 3.5 GHz, respectively. The maximum gain at the resonant frequency of 2.45 and 3.5 GHz are 9.3 and 11.33 dBi, respectively.

Keywords: multi-slotted antenna, microstrip patch antenna, frequency selective surface, artificial magnetic conduction

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Authors: Pan Hongxia, Wang Zhenhua

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In this paper, the EMD decomposition in the process of endpoint effect adopted data based on AR model to predict the continuation and window function method of combining the two effective inhibition. Proven by simulation of the simulation signal obtained the ideal effect, then, apply this method to the gearbox test data is also achieved good effect in the process, for the analysis of the subsequent data processing to improve the calculation accuracy. In the end, under various working conditions for the gearbox fault diagnosis laid a good foundation.

Keywords: gearbox, fault diagnosis, ar model, end effect

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Authors: Faisal A. Salih

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Verapamil hydrochloride (Ver) is a drug used in medicine for arrythmia, angina and hypertension as a calcium channel blocker. For the quantitative determination of Ver in dosage forms, the HPLC method is most often used. A convenient alternative to the chromatographic method is potentiometry using a Verselective electrode, which does not require expensive equipment, can be used without separation from the matrix components, which significantly reduces the analysis time, and does not use toxic organic solvents, being a "green", "environmentally friendly" technique. It has been established in this study that the rational choice of the membrane plasticizer and the preconditioning and measurement algorithms, which prevent nonexchangeable extraction of Ver into the membrane phase, makes it possible to achieve excellent analytical characteristics of Ver-selective electrodes based on commercially available components. In particular, an electrode with the following membrane composition: PVC (32.8 wt %), ortho-nitrophenyloctyl ether (66.6 wt %), and tetrakis-4-chlorophenylborate (0.6 wt % or 0.01 M) have the lower detection limit 4 × 10−8 M and potential reproducibility 0.15–0.22 mV. Both direct potentiometry (DP) and potentiometric titration (PT) methods can be used for the determination of Ver in tablets and injection solutions. Masses of Ver per average tablet weight determined by the methods of DP and PT for the same set of 10 tablets were (80.4±0.2 and80.7±0.2) mg, respectively. The masses of Ver in solutions for injection, determined by DP for two ampoules from one set, were (5.00±0.015 and 5.004±0.006) mg. In all cases, good reproducibility and excellent correspondence with the declared quantities were observed.

Keywords: verapamil, potentiometry, ion-selective electrode, pharmaceutical analysis

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Authors: Kien Xuan Ngo

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Cassiicolin (Cas), a toxin produced by Corynespora cassiicola, is responsible for corynespora leaf fall (CLF) disease in rubber trees. Currently, the molecular mechanism of the cytotoxicity of Cas isoforms (i.e., Cas1, Cas2) on rubber leaves and its host selectivity have not been fully elucidated. This study analyzed the binding of Cas1 and Cas2 to membranes consisting of different plant lipids and their membrane-disruption activities. Using high-speed atomic force microscopy and confocal microscopy, this study reveals that the binding and disruption activities of Cas1 and Cas2 on lipid membranes are strongly dependent on the specific plant lipids. The negative phospholipids, glycerolipids, and sterols are more susceptible to membrane damage caused by Cas1 and Cas2 than neutral phospholipids and betaine lipids. In summary, This study unveils that (i) Cas1 and Cas2 directly damage and cause necrosis in the leaves of specific rubber clones; (ii) Cas1 and Cas2 can form biofilm-like structures on specific lipid membranes (negative phospholipids, glycerolipids, and sterols). The biofilm-like formation of Cas toxin plays an important role in selective disruption on lipid membranes; (iii) Vulnerability of the specific cytoplasmic membranes to the selective Cas toxin is the most remarkable feature of cytotoxicity of Cas toxin on plant cells. Finally, researcher’s exploration is crucial to understand the basic molecular mechanism underlying the host-selective toxic interaction of Cas toxin with cytoplasmic membranes in plant cells.

Keywords: cassiicolin, corynespora leaf fall disease, high-speed AFM, giant liposome vesicles

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Authors: M. S. Hasni, J. Guan, K. Yakimchuk, M. Berglund, B. Sander, G. Enblad, R. M. Amini, S. Okret

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Lymphomas are generally not considered as endocrine-related cancers. However, most lymphoid malignancies show gender differences in incidence and show prognosis with males being more affected. Furthermore, some epidemiological data indicate a protective role of estrogens against Non-Hodgkin lymphomas. Recent studies have demonstrated estrogen receptor β (ERβ) to be the major ER expressed in normal and malignant cells of lymphoid origin. We have analyzed the effects of estradiol and selective ERα and ERβ agonists on lymphoma growth in culture and in vivo. Treating lymphoma cells with estradiol or ERα selective agonist had minor or no effect on cell growth while selective ERβ agonist treatment showed an antiproliferative effect. When grafting mice with murine T lymphoma cells, male mice developed larger tumors compared to female mice, a difference that was abolished following ovariectomy, demonstrating estrogen-dependent growth in vivo. When subcutaneously grafting lymphoma cells to mice, so far growth of all tested human B lymphoma tumors (Raji and Ramos Burkitt lymphoma, SU.DHL4 (GC) and U2932 (ABC) DLBCL, Granta-519, Maver1 and Z138 MCL cells), were reduced following treatment with ERβ selective agonist (ref. 2 and unpublished). Moreover, the number and size of liver foci of disseminating Raji cells was reduced. We have identified target genes and mechanism that could explain the above effects of ERβ agonists. This included effects on angio and lymphangiogenesis. Now we have further analyzed effects of ERβ agonists on Ibrutinib-sensitive and -insensitive MCL cells in xenograft experiments as well as ERβ expression in primary lymphoma material (DLBCL). Preliminary statistical analysis has been done correlating ERβ expression to other biomarkers and clinical data.

Keywords: lymphomas, estrogen receptors, cancer, liver foci

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Authors: Imran Muhammad

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The main cause of infectious disease in the modern world is Mycobacterium Tuberculosis (MT). To combat tuberculosis, new and efficient drugs are an urgent need in the modern world. Schif bases are potent for their biological pharmacophore activity. Thus we selected different Vanillin-based Schiff bases for their binding activity against target enzymes of Mycobacterium tuberculosis that is (DprE1 (decaprenyl phosphoryl-β-D-ribose 2′-epimerase), and DNA gyrase subunit-A), using molecular docking. We evaluate the inhibition potential, interaction, and binding mode of these compounds with the target enzymes.

Keywords: schiff bases, tuberculosis, DNA gyrase, DprE1, docking

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Authors: Hui Liu, Xiaozan Wang, Jiarong Zhong, Ziming Shao

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Introduction: Related research shows that students don’t concentrate on teacher’s speaking in the classroom. The d2 attention test is a time-limited test about selective attention. The d2 attention test can be used to evaluate individual selective attention. Purpose: To use the d2 attention test tool to measure the difference between the attention level of the experimental class and the control class before and after Brain-Break and to explore the effect of Brain-Break in the classroom on students' selective attention. Methods: According to the principle of no difference in pre-test data, two classes in the fourth- grade of Shenzhen Longhua Central Primary School were selected. After 20 minutes of class in the third class in the morning and the third class in the afternoon, about 3-minute Brain-Break intervention was performed in the experimental class for 10 weeks. The normal class in the control class did not intervene. Before and after the experiment, the d2 attention test tool was used to test the attention level of the two-class students. The paired sample t-test and independent sample t-test in SPSS 23.0 was used to test the change in the attention level of the two-class classes around 10 weeks. This article only presents results with significant differences. Results: The independent sample t-test results showed that after ten-week of Brain-Break, the missed errors (E1 t = -2.165 p = 0.042), concentration performance (CP t = 1.866 p = 0.05), and the degree of omissions (Epercent t = -2.375 p = 0.029) in experimental class showed significant differences compared with control class. The students’ error level decreased and the concentration increased. Conclusions: Adding Brain-Break interventions in the classroom can effectively improve the attention level of fourth-grade primary school students to a certain extent, especially can improve the concentration of attention and decrease the error rate in the tasks. The new sport's learning model is worth promoting

Keywords: cultural class, micromotor, attention, D2 test

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Authors: Matthew Omoniyi Adebola, Jude E Amadi

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Ground nut (Arachis hypogaea) is one of the most popular commercial crops in Nigeria. Its suc-cessful production has been drastically affected by early leaf spot disease caused by Mycosphae-rella arachidis Deighton. In vitro control of the pathogen by six medicinal plants (Entada afri-cana, Vitex doniana, Lawsonia inermis, Azadirachta indica, Acalypha hispida and Nuaclea lati-folia) was assessed in this study. The extracts of the plants were prepared using cold and hot wa-ter and alcohol. The pathogen was isolated from ground nut infected with early leaf spot disease. The results revealed a great significant difference (P<0.05) in yield of extracts between cold water, hot water, and alcohol extracts. A significant difference (P<0.05) was observed in percentage concentrations of the various phytochemical constituents present in the extracts. Flavonoids per-centage concentration was the highest (0.68 - 1.95%) followed by saponnin(0.09-1.53%) in N. latifolia extracts. Steroiods had the least percentage concentrations (0.00- 0.09%)followed by terpenoids(0.02–0.71%) and proanthocyannin (0.05 – 0.86%). N. latifolia extracts produced the highest percentage concentrations (0.07–1.95%) of all the phytochemicals followed by A. indi-ca(0.05–1.64%)and least concentrations were obtained in A. hispidia(0.09 – 0.87%)and V. do-niana (0.00–0.88%). The extracts inhibited spore germination and growth of M. arachidis. The inhibition by alcohol extracts was high and significantly different (P>0.05) from cold and hot water extracts. Alcohol extract of L. inermis gave 100% spore germination inhibition followed by N. latifolia and A.indica with 97.75% and 85.60% inhibition respectively. Therefore, field trials of these six medicinal plants on the control of early leaf spot disease of ground nut are rec-ommended.

Keywords: groundnut, phytochemicals, medicinal plants, extracts, inhibition

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Authors: Temesgen Geremew

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The excessive emission of heavy metal ions from industrial processes poses a serious threat to both the environment and human health. This study presents a distinct approach utilizing (PTh-MnS/CoS NPs) for the highly selective and sensitive detection of Hg²⁺ ions in water. Such detection is crucial for safeguarding human health, protecting the environment, and accurately assessing toxicity. The fabrication method employs a simple and efficient chemical precipitation technique, harmoniously combining polythiophene, MnS, and CoS NPs to create highly active substrates for SERS. The MnS@Hg²⁺ exhibits a distinct Raman shift at 1666 cm⁻¹, enabling specific identification and demonstrating the highest responsiveness among the studied semiconductor substrates with a detection limit of only 1 nM. This investigation demonstrates reliable and practical SERS detection for Hg²⁺ ions. Relative standard deviation (RSD) ranged from 0.49% to 9.8%, and recovery rates varied from 96% to 102%, indicating selective adsorption of Hg²⁺ ions on the synthesized substrate. Furthermore, this research led to the development of a remarkable set of substrates, including (MnS, CoS, MnS/CoS, and PTh-MnS/CoS) nanoparticles were created right there on SiO₂/Si substrate, all exhibiting sensitive, robust, and selective SERS for Hg²⁺ ion detection. These platforms effectively monitor Hg²⁺ concentrations in real environmental samples.

Keywords: surface-enhanced raman spectroscopy (SERS), sensor, mercury ions, nanoparticles, and polythiophene.

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Authors: Hany M. Abd El-Lateef

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Two novel Schiff bases, 5-bromo-2-[(E)-(pyridin-3-ylimino) methyl] phenol (HBSAP) and 5-bromo-2-[(E)-(quinolin-8-ylimino) methyl] phenol (HBSAQ) have been synthesized. They have been characterized by elemental analysis and spectroscopic techniques (UV–Vis, IR and NMR). Moreover, the molecular structure of HBSAP and HBSAQ compounds are determined by single crystal X-ray diffraction technique. The inhibition activity of HBSAP and HBSAQ for carbon steel in 3.5 %NaCl+0.1 M HCl for both short and long immersion time, at different temperatures (20-50 ºC), was investigated using electrochemistry and surface characterization. The potentiodynamic polarization shows that the inhibitors molecule is more adsorbed on the cathodic sites. Its efficiency increases with increasing inhibitor concentrations (92.8 % at the optimal concentration of 10-3 M for HBSAQ). Adsorption of the inhibitors on the carbon steel surface was found to obey Langmuir’s adsorption isotherm with physical/chemical nature of the adsorption, as it is shown also by scanning electron microscopy. Further, the electronic structural calculations using quantum chemical methods were found to be in a good agreement with the results of the experimental studies.

Keywords: carbon steel, Schiff bases, corrosion inhibition, SEM, electrochemical techniques

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Authors: N. Kazantseva, P. Krakhmalev, I. Yadroitsev, A. Fefelov, N. Vinogradova, I. Ezhov, T. Kurennykh

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Martensitic texture-phase transition in Selective Laser Melting (SLM) Ti-6Al-4V (ELI) alloys was found. Electron Backscatter Diffraction (EBSD) analysis showed the initial cubic beta < 100 > (001) BCC texture. Such kind of texture is observed in BCC metals with flat rolling texture when axis is in the direction of rolling and the texture plane coincides with the plane of rolling. It was found that the texture of the parent BCC beta-phase determined the texture of low-temperature HCP alpha-phase limited the choice of its orientation variants. The {10-12} < -1011 > twinning system in titanium alloys after SLM was determined. Analysis of the oxygen contamination in SLM alloys was done. Comparison of the obtained results with the conventional titanium alloys is also provided.

Keywords: additive technology, texture, twins, Ti-6Al-4V, oxygen content

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Authors: Elizabeth Loza-Valerdi, Victor Pardiñas-Rios, Arnulfo Pluma-Pluma, Andres Breton-Toral, Julio Cercado-Jaramillo

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The purification processes for mixtures of isomeric monosaccharides using industrial chromatographic methods poses a serious technical challenge. Mixtures of 2 or 3 monosaccharides are difficult to separate by strictly physical or chemical techniques. Differential fermentation by microbial cultures is an increasingly interesting way of selective enrichment in a particular kind of monosaccharides when a mixture of them is present in the solution, and only one has economical value. Osmotolerant yeast cultures provide an interesting source of biocatalysts for the selective catabolism of monosaccharides in media containing high concentrations of total soluble sugars. A collection of 398 yeast strains has been obtained using endemic and unique sources of fruit juices, industrial syrups, honey, and other high sugar content substrates, either natural or man made, products and by-products from Mexico. The osmotolerance of the strains was assessed by plate assay both in glucose (20-40-60%w/w). Strains were classified according to their osmotolerance in low, medium or highly tolerant to high glucose concentrations. The purified cultures were tested by their ability to growth in a solid plate media or liquid media of Yeas Nitrogen Base (YNB), added with specific monosaccharides as sole carbon source (glucose, galactose, lactose and fructose). Selected strains were subsequently tested in fermentation experiments with mixtures of two monosaccharides (galactose/glucose and glucose/fructose). Their ability to grow and selectively catabolize one monosaccharide was evaluated. Growth, fermentation activity and products of metabolism were determined by plate counts, CO2 production, turbidity and chromatographic analysis by HPLC. Selective catabolism of one monosaccharide in liquid media containing two monosaccharides was confirmed for 8 strains. Ion Exchange chromatographic processes were used in production of high fructose or galactose syrup. Laboratory scale processes for the production of fructose or galactose enriched syrups is now feasible, with important applications in food (like high fructose syrup as edulcorant) and fermentation technology (for GOS production).

Keywords: osmotolerant yeasts, selective metabolism, fructose syrup, GOS

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

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

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

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Authors: H. Minor-Pérez, A. M. Mota-Silva, S. Ortiz-Barrios

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Substances of vegetable origin with antioxidant capacity have a high potential for application on the conservation of some foods, can prevent or reduce for example oxidation of lipids. However a food is a complex system whose wide variety of components wich can reduce or eliminate this antioxidant capacity. The antioxidant activity can be determined with the ABTS technique. The radical ABTS+ is generated from the acid 2, 2´ - Azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS). This radical is a composite color bluish-green, stable and with a spectrum of absorption into the UV-visible. The addition of antioxidants causes discoloration, value that can be reported as a percentage of inhibition of the cation radical ABTS+. The objective of this study was evaluated the effect of the combination of the pH and the essential oil of cinnamon (EOC) on inhibition of the radical ABTS+, using statistical design of central point (Design Expert) to obtain mathematical models that describe this phenomenon. Were evaluated 17 treatments with combinations of pH 5, 6 and 7 (citrate-phosphate buffer) and the concentration of essential oil of cinnamon (C): 0 µg/mL, 100 µg/mL and 200 µg/mL. The samples were analyzed using the ABTS technique. The reagent was dissolved in methanol 80% to standardized the absorbance to 0.7 +/- 0.1 at 754 nm. Then samples were mixed with reagent standardized ABTS and after 1 min and 7 min absorbance was read for each treatment at 754 nm. Was used a curve pattern with vitamin C and reported the values as inhibition (%) of radical ABTS+. The statistical analysis shows the experimental results were adjusted to a quadratic model, to the times of 1 min and 7 min. This model describes the influence of the factors investigated independently: pH and cinnamon essential oil (µg/mL) and the effect of the interaction between pH*C, as well as the square of the pH2 and C2. The model obtained was Y = 10.33684 - 3.98118*pH + 1.17031*C + 0.62745*pH2 - 3.26675*10-3*C2 - 0.013112*pH*C, where Y is the response variable. The coefficient of determination was 0.9949 for 1 min. The equation was obtained at 7 min and = - 10.89710 + 1.52341*pH + 1.32892*C + 0.47953*pH2 - 3.56605*10- *C2 - 0.034687*pH*C. The coefficient of determination was 0.9970. This means that only 1% of the total variation is not explained by the developed models. At 100 µg/mL of EOC was obtained an inhibition percentage of 80%, 84% and 97% for the pH values of 5,6 and 7 respectively, while a value of 200 µg/mL the inhibition (%) was very similar for the treatments. In these values of pH was obtained an inhibition close 97%. In conclusion the pH does not have a significant effect on the antioxidant capacity, while the concentration of EOC was decisive for the antioxidant capacity. The authors acknowledge the funding provided by the CONACYT for the project 131998.

Keywords: antioxidant activity, ABTS technique, essential oil of cinnamon, mathematical models

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