Search results for: dual inhibitors

Authors: Jaskarn Singh Bhullar, Divya Taneja, Manish Gupta, Rajesh Kumar Narula

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The existence conditions of dual containing constacyclic codes have opened a new path for finding quantum maximum distance separable (MDS) codes. Using these conditions parameters of length n=(q²+1)/2 quantum MDS codes were improved. A class of quantum MDS codes of length n=(q²+q+1)/h, where h>1 is an odd prime, have also been constructed having large minimum distance and these codes are new in the sense as these are not available in the literature.

Keywords: hermitian construction, constacyclic codes, cyclotomic cosets, quantum MDS codes, singleton bound

Procedia PDF Downloads 385

Authors: Puji Sucia Sukmaningrum, Achsania Hendratmi, Noven Suprayogi, Muhammad Madyan

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Theoretically, Islamic banks in Indonesia and Malaysia not necessarily aware to the interest rate fluctuation, since they don’t use interest-based instruments. Both countries use dual banking system in which Islamic and conventional banking system are exist. This situation makes the profit-sharing level of the Islamic banks will be indirectly affected by the interest rate fluctuation from the conventional banks system. One of the risk management tools for anticipating the risk of interest rate fluctuation is gap management, which has purpose to narrow the difference between Rate Sensitive Asset (RSA) and Rate Sensitive Liability (RSL). This formed gap will give the information about the risk potential in Islamic banks which respect to the fluctuation on the interest rate. This study aims to determine the position of the gap formed at Islamic Maybank Indonesia and Islamic Maybank Malaysia, and analyze the difference in the formation of gap based on the period of sensitivity. This study is a quantitative research with comparative study using sensitivity gap analysis, independent sample t-test, and Mann-Whitney method. The data being used was secondary data from Maturity Profile contained in the Annual Financial Report of Islamic Maybank Indonesia and Islamic Maybank Malaysia from 2011 to 2015 period. The result shows that, cumulatively the formation of the gap was negative gap. From the results of independent sample t-test and Mann-Whitney, the formation of the gap in Islamic Maybank Indonesia and Islamic Maybank Malaysia for a period of sensitivity of ≤ 1 month and >1-3 months show a significant difference, while the period of sensitivity >3-12 months does not. The result shows, even though Indonesia and Malaysia using same dual banking systems, the gap values are different. The difference in debt policy between Indonesia and Malaysia also affecting the gap sensitivity in debt. In can be concluded that each country needs an appropriate gap management to support its Islamic banking performance specifically.

Keywords: assets and liability management, gap management, interest rate risk, Islamic bank

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Authors: Talha Ali Khan

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Discovering different energy resources to full fill the world growing demand is now one of the society’s bigger challenge for the next half-century. The main task is to convert the sun radiation into electricity via photovoltaic solar cells which is suddenly decreasing $/watt of delivered solar electricity. Therefore, in this context, the sun trackers are those devices that can be used to ameliorate efficiency. In this paper, a variety of the sun tracking systems are evaluated and their merits and demerits are highlighted. The most adept and proficient sun-tracking devices are polar axis and azimuth-elevation types.

Keywords: dual axis, fixed axis, sun tracker, MPPT

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Authors: Pervaiz Ahmad, Mayeen Uddin Khandaker, Yusoff Mohd Amin

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A unique cone-like morphologies of boron nitride microtubes with larger internal space and thin walls structure are synthesized in a dual zone quartz tube furnace at 1200 ° C with ammonia as a reaction atmosphere. The synthesized microtubes are found to have diameter in the range of 1 to ̴ 2 μm with walls thickness estimated from 10 – 100 nm. XPS survey shows N 1s and B 1s peaks at 398.7 eV and 191 eV that represent h-BN in the sample. Raman spectroscopy indicates a high intensity peak at 1372.53 (cm-1) that corresponds to the E2g mode of h-BN.

Keywords: BNMTs, synthesis, reaction atmosphere, growth

Procedia PDF Downloads 382

Authors: İsmail Çeli̇k, Gülgün Ayhan-Kılcıgi̇l, Arzu Onay-Beşi̇kçi̇

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In this study, some 2-(2-phenyl/substitutedphenyl)- lH-benzo[d]'imidazol-l-yl)-N'-(alkylthiosemicarbazide were designed and prepared. Firstly, 2-phenyl/ suhstitutedphenyl-lH-Benzo[d]imidazole was prepared via oxidative condensation of o-phenylenediamine, benzaldehyde and sodium metabisulfite. Treatment of the benzimidazole compound with ethyl chloroacetate in KOH/DMSO gave the ester compound ethyl 2-(2-substitutedphenyl)-1H-benzo[d]imidazol-l-yl)acetate. Hydrazine hydrate and the ester in ethanol were refluxed for 4 h to give 2-(2-phenyl/substitutedphenyl)-1H-benzo[d]imidazol-l-yl)acetohydrazide. Thiosemicarbazides were obtained by condensing acyl hydrazide with the alkylisothiocyanate in ethanol. Following the structure elucidation, benzimidazole compounds were tested for their EGFR kinase inhibitory activities by using ADP-GloTM Kinase Assay.

Keywords: benzimidazole, EGFR kinase inhibitor, synthesis, thiosemicarbazide

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Authors: Talha Ali Khan

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Discovering different energy resources to fulfill the world's growing demand is now one of the society’s bigger challenges for the next half-century. The main task is to convert the sun radiation into electricity via photovoltaic solar cells which is suddenly decreasing $/watt of delivered solar electricity. Therefore, in this context the sun trackers are those devices that can be used to ameliorate efficiency. In this paper, a variety of the sun tracking systems are evaluated and their merits and demerits are highlighted. The most adept and proficient sun-tracking devices are polar axis and azimuth-elevation types.

Keywords: dual axis, fixed axis, sun tracker, sun radiation

Procedia PDF Downloads 453

Authors: T. Benyetho, L. El Abdellaoui, J. Terhzaz, H. Bennis, N. Ababssi, A. Tajmouati, A. Tribak, M. Latrach

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This work presents a new planar multiband antenna based on fractal geometry. This structure is optimized and validated into simulation by using CST-MW Studio. To feed this antenna we have used a CPW line which makes it easy to be incorporated with integrated circuits. The simulation results presents a good matching input impedance and radiation pattern in the GSM band at 900 MHz and ISM band at 2.4 GHz. The final structure is a dual band fractal antenna with 70 x 70 mm² as a total area by using an FR4 substrate.

Keywords: Antenna, CPW, fractal, GSM, multiband

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Authors: P. Saha, R. Ganguly, N. K .Singha, A. Pich

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Microgel, a smart class of material, has drawn attention in the past few years due to its response to external stimuli like temperature, pH, and ionic strength of the solution. Among them, one type of polymer becomes soluble, and the other becomes insoluble in water upon heating displaying upper critical solution temperature (UCST) (e.g., polysulfobetaine, PSB) and lower critical solution temperature (LCST) (e.g., poly(N-vinylcaprolactam, PVCL)) respectively. Polyzwitterions, electrically neutral polymers are biocompatible, biodegradable, and non-cytotoxic in nature, and presence of zwitterionic pendant group in the main backbone makes them stable against temperature and pH variations and strong hydration capability in salt solution promotes them to be used as interfacial bio-adhesion resistance material. Majority of zwitterionic microgels have been synthesized in mini- emulsion technique using free radical polymerization approach. Here, a new route to synthesize dual thermo-responsive PVCL microgels decorated with appreciable amount of zwitterionic PSB chains was developed by a purely water-based surfactant-free reversible addition–fragmentation chain transfer (RAFT) precipitation polymerization. PSB macro-RAFTs having different molecular weights were synthesized and utilized for surface-grafting with PVCL microgels varying the macro-RAFT concentration using N,N′-methylenebis(acrylamide) (BIS) as cross-linker. Increasing the PSB concentration in the PVCL microgels resulted in a linear increase in UCST but decrease in hydrodynamic radius due to strong intrachain coulombic attraction forces acting between the opposite charges present in the zwitterionic groups. Anti- fouling effect was observed on addition of BSA protein solution on the microgel-coated membrane surfaces as studied by fluorescence spectrophotoscopy.

Keywords: microgels, polyzwitterions, upper critical solution temperature-lower critical solution temperature, UCST-LCST, ionic crosslinking

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Authors: Muhammad Qamar Masood, Syed Abbas Raza, Umar Yousaf Raja, Imran Hassan, Bilal Afzal, Muhammad Aleem Zahir, Atika Shaheer

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Background: Cardiovascular disease (CVD) is a major burden among people with type 2 diabetes (T2D) with 1 in 3 reported to have CVD. Therefore, understanding real-world clinical characteristics and prescribing patterns could help in better care. Objective: The CONVERGE (Cardiovascular Outcomes and Value in the Real world with GLP-1RAs) study characterized demographics and medication usage patterns in T2D intensified (add-on to metformin) overall population. The data were further divided into subgroups {dipeptidyl peptidase-4 inhibitors (DPP-4is), sulfonylureas (SUs), insulins, glucagon-like peptide-1 receptor agonists (GLP-1 RAs) and sodium-glucose cotransporter-2 inhibitors (SGLT-2is)}, according to the latest prescribed antidiabetic agent (ADA) in India/Pakistan/Thailand. Here, we report findings from Pakistan. Methods: A multi-center retrospective study utilized data from medical records between 13-Sep-2008 (post-market approval of GLP-1RAs) and 31-Dec-2017 in adults (≥18-year-old). The data for this study were collected from 05 centers / institutes located in major cities of Pakistan, including Karachi, Lahore, Islamabad, and Multan. These centers included National Hospital, Aga Khan University Hospital, Diabetes Endocrine Clinic Lahore, Shifa International Hospital, Mukhtar A Sheikh Hospital Multan. Data were collected at start of medical record and at 6 or 12-months prior to baseline based on variable type; analyzed descriptively. Results: Overall, 1,010 patients were eligible. At baseline, overall mean age (SD) was 51.6 (11.3) years, T2D duration was 2.4 (2.6) years, HbA1c was 8.3% (1.9) and 35% received ≥1CVD medications in the past 1-year (before baseline). Most frequently prescribed ADAs post-metformin were DPP-4is and SUs (~63%). Only 6.5% received GLP-1RAs and SGLT-2is were not available in Pakistan during the study period. Overall, it took a mean of 4.4 years and 5 years to initiate GLP-1RAs and SGLT-2is, respectively. In comparison to other subgroups, more patients from GLP-1RAs received ≥3 types of ADA (58%), ≥1 CVD medication (64%) and had higher body mass index (37kg/m2). Conclusions: Utilization of GLP-1RAs and SGLT-2is was low, took longer time to initiate and not before trying multiple ADAs. This may be due to lack of evidence for CV benefits for these agents during the study period. The planned phase 2 of the CONVERGE study can provide more insights into utilization and barriers to prescribe GLP-1RAs and SGLT-2is post 2018 in Pakistan.

Keywords: type 2 diabetes, GLP-1RA, treatment intensification, cardiovascular disease

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Authors: Nurjannatul Naim Kamaruddin, Tengku Sifziuzl Tengku Muhammad, Aina Farahiyah Abdul Manan, Habsah Mohamad

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Atherosclerosis which leads to cardiovascular diseases such as myocardial infarction, unstable angina (ischemic heart pain), sudden cardiac death and stroke is the principal cause of death worldwide. It has been a very critical issue as current common drug treatment, statin therapy has left bad side effects like rhabdomyolysis, atrial fibrillation, liver disease, abdominal and chest pain. Interestingly, the discoveries of proprotein convertase subtilisin-kexin type 9 have paved a new way in the treatment of atherosclerosis. This serine protease is believed to involve in the regulation of LDL- uptake by LDL-receptor. Therefore, this study was conducted to evaluate the potential of Acanthaster plancii fractions to reduce the transcriptional activity of the PCSK9 promoter. In this study, the marine organism which is Acanthaster plancii has been used as the source for marine compounds in inhibiting PCSK9. The cytotoxicity activity of ten fractions from the methanol extracts of Acanthaster plancii was investigated on HepG2 cell lines using MTS assay and dual glo luciferase assay was carried out later to analyses the effects of the samples in reducing the transcriptional activity of the PCSK9 promoter. Both assays used fractions with five different concentrations, 3.13µg/mL, 6.25µg/mL, 12.5µg/mL, 25µg/mL, and 50µg/mL. MTS assay indicated that the fractions are non-cytotoxic towards HepG2 cell lines as their IC50 value is greater than 30µg/mL. Whilst, for the dual glo luciferase assay, among all the fractions, Enhance Fraction 2 (EF2) showed the best potential in reducing the transcriptional activity of the PCSK9 promoter. The results indicated that this EF2 gave the lowest PCSK9 promoter expression at low concentration which is 0.2 fold change at 6.25µg/mL. This finding suggested that further analysis should be done to validate the potential of Acanthaster plancii as the source of anti-atherosclerotic agent.

Keywords: Acanthaster plancii, atherosclerosis, luciferase assay, PCSK9

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Authors: Lachin Mikjtarnejad, Mohsen Farzaneh

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Various microbes, such as fungi and bacteria species, are naturally found in the fruit microbiota, and some of them act as a pathogen and result in fruit rot. Among non-pathogenic microbes, yeasts (single-celled microorganisms belonging to the fungi kingdom) can colonize fruit tissues and interact with them without causing any damage to them. Although yeasts are part of the plant microbiota, there is little information about their interactions with plants in comparison with bacteria and filamentous fungi. According to several existing studies, some yeasts can colonize different plant species and have the biological control ability to suppress some of the plant pathogens. It means those specific yeast-colonized plants are more resistant to some plant pathogens. The major objective of the present investigation is to isolate yeast strains from apple fruit and screen their ability to control Penicillium expansum, the causal agent of blue mold of fruits. In the present study, psychrotrophic and epiphytic yeasts were isolated from apple fruits that were stored at low temperatures (0–1°C). Totally, 42 yeast isolates were obtained and identified by molecular analysis based on genomic sequences of the D1/D2 and ITS1/ITS4 regions of their rDNA. All isolated yeasts were primarily screened by' in vitro dual culture assay against P. expansum by measuring the fungus' relative growth inhibition after 10 days of incubation. The results showed that the mycelial growth of P. expansum was reduced between 41–53% when challenged by promising yeast strains. The isolates with the strongest antagonistic activity belonged to Metschnikowia pulcherrima A13, Rhodotorula mucilaginosa A41, Leucosporidium Scottii A26, Aureobasidium pullulans A19, Pichia guilliermondii A32, Cryptococcus flavescents A25, and Pichia kluyveri A40. The results of seven superior isolates to inhibit blue mold decay on fruit showed that isolates A. pullulans A19, L. scottii A26, and Pi. guilliermondii A32 could significantly reduce the fruit rot and decay with 26 mm, 22 mm and 20 mm zone diameter, respectively, compared to the control sample with 43 mm. Our results show Pi. guilliermondii strain A13 was the most effective yeast isolates in inhibiting P. expansum on apple fruits. In addition, various biological control mechanisms of promising biological isolates against blue mold have been evaluated to date, including competition for nutrients and space, production of volatile metabolites, reduction of spore germination, production of siderophores and production of extracellular lytic enzymes such as chitinase and β-1,3-glucanase. However, the competition for nutrients and the ability to inhibit P. expansum spore growth have been introduced as the prevailing mechanisms among them. Accordingly, in our study, isolates A13, A41, A40, A25, A32, A19 and A26 inhibited the germination of P. expansum, whereas isolates A13 and A19 were the strongest inhibitors of P. expansum mycelia growth, causing 89.13% and 81.75 % reduction in the mycelial surface, respectively. All the promising isolates produced chitinase and β-1,3-glucanase after 3, 5 and 7 days of cultivation. Finally, based on our findings, we are proposing that, Pi. guilliermondiias as an effective biocontrol agent and alternative to chemical fungicides to control the blue mold of apple fruit.

Keywords: yeast, yeast enzymes, biocontrol, post harvest diseases

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Authors: Jia Li, Xing Wei, Yuchen Hong, Yang Lu

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Detecting vehicle behavior has always been the focus of intelligent transportation, but with the explosive growth of the number of vehicles and the complexity of the road environment, the vehicle behavior videos captured by traditional surveillance have been unable to satisfy the study of vehicle behavior. The traditional method of manually labeling vehicle behavior is too time-consuming and labor-intensive, but the existing object detection and tracking algorithms have poor practicability and low behavioral location detection rate. This paper proposes a vehicle behavior detection algorithm based on the dual-stream convolution network and the multi-dimensional video dynamic detection network. In the videos, the straight-line behavior of the vehicle will default to the background behavior. The Changing lanes, turning and turning around are set as target behaviors. The purpose of this model is to automatically mark the target behavior of the vehicle from the untrimmed videos. First, the target behavior proposals in the long video are extracted through the dual-stream convolution network. The model uses a dual-stream convolutional network to generate a one-dimensional action score waveform, and then extract segments with scores above a given threshold M into preliminary vehicle behavior proposals. Second, the preliminary proposals are pruned and identified using the multi-dimensional video dynamic detection network. Referring to the hierarchical reinforcement learning, the multi-dimensional network includes a Timer module and a Spacer module, where the Timer module mines time information in the video stream and the Spacer module extracts spatial information in the video frame. The Timer and Spacer module are implemented by Long Short-Term Memory (LSTM) and start from an all-zero hidden state. The Timer module uses the Transformer mechanism to extract timing information from the video stream and extract features by linear mapping and other methods. Finally, the model fuses time information and spatial information and obtains the location and category of the behavior through the softmax layer. This paper uses recall and precision to measure the performance of the model. Extensive experiments show that based on the dataset of this paper, the proposed model has obvious advantages compared with the existing state-of-the-art behavior detection algorithms. When the Time Intersection over Union (TIoU) threshold is 0.5, the Average-Precision (MP) reaches 36.3% (the MP of baselines is 21.5%). In summary, this paper proposes a vehicle behavior detection model based on multi-dimensional dynamic detection network. This paper introduces spatial information and temporal information to extract vehicle behaviors in long videos. Experiments show that the proposed algorithm is advanced and accurate in-vehicle timing behavior detection. In the future, the focus will be on simultaneously detecting the timing behavior of multiple vehicles in complex traffic scenes (such as a busy street) while ensuring accuracy.

Keywords: vehicle behavior detection, convolutional neural network, long short-term memory, deep learning

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Authors: Razieh Niazmand, Dina Sadat Mousavian, Parvin Sharayei

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This study investigated the effect of carboxymethyl cellulose (CMC), tragacanth, and saalab hydrocolloids in two concentrations (0.3%, 0.7%) and different frying media, refined canola oil (RCO), RCO + 1% bene kernel oil (BKO), and RCO + 1 mg/l unsaponifiable matter (USM) of BKO on acrylamide formation in fried potato slices. The hydrocolloid coatings significantly reduced acrylamide formation in potatoes fried in all oils. Increasing the hydrocolloid concentration from 0.3% to 0.7% produced no effective inhibition of acrylamide. The 0.7 % CMC solution was identified as the most promising inhibitor of acrylamide formation in RCO oil, with a 62.9% reduction in acrylamide content. The addition of BKO or USM to RCO led to a noticeable reduction in the acrylamide level in fried potato slices. The findings suggest that a 0.7% CMC solution and RCO+USM are promising inhibitors of acrylamide formation in fried potato products.

Keywords: CMC, frying, potato, saalab, tracaganth

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Authors: Hercules Argyropoulos, Thomas F. Johnson, Nigel B Jackson, Kalliopi Zourna, Daniel G. Bracewell

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Lipid encapsulation has become essential in drug delivery, notably for mRNA vaccines during the COVID-19 pandemic. However, their sterile filtration poses challenges due to the risk of deformation, filter fouling and product loss from adsorption onto the membrane. Choosing the right filtration membrane is crucial to maintain sterility and integrity while minimizing product loss. The objective of this study is to develop a rigorous analytical framework utilizing confocal microscopy and filtration blocking models to elucidate the fouling mechanisms of liposomes as a model system for this class of delivery vehicle during sterile filtration, particularly in response to variations in transmembrane pressure (TMP) during the filtration process. Experiments were conducted using fluorescent Lipoid S100 PC liposomes formulated by micro fluidization and characterized by Multi-Angle Dynamic Light Scattering. Dual-layer PES/PES and PES/PVDF membranes with 0.2 μm pores were used for filtration under constant pressure, cycling from 30 psi to 5 psi and back to 30 psi, with 5, 6, and 5-minute intervals. Cross-sectional membrane samples were prepared by microtome slicing and analyzed with confocal microscopy. Liposome characterization revealed a particle size range of 100-140 nm and an average concentration of 2.93x10¹¹ particles/mL. Goodness-of-fit analysis of flux decline data at varying TMPs identified the intermediate blocking model as most accurate at 30 psi and the cake filtration model at 5 psi. Membrane resistance analysis showed atypical behavior compared to therapeutic proteins, with resistance remaining below 1.38×10¹¹ m⁻¹ at 30 psi, increasing over fourfold at 5 psi, and then decreasing to 1-1.3-fold when pressure was returned to 30 psi. This suggests that increased flow/shear deforms liposomes enabling them to more effectively navigate membrane pores. Confocal microscopy indicated that liposome fouling mainly occurred in the upper parts of the dual-layer membrane.

Keywords: sterile filtration, membrane resistance, microfluidization, confocal microscopy, liposomes, filtration blocking models

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Authors: Oseyemi O. Olubomehin, Edith O. Ajaiyeoba, Kio A. Abo, Eleonora D. Goosen

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Diabetes is a major degenerative disease of global concern and it is the third most lethal disease of mankind, accounting for about 3.2 million deaths annually. Lowering postprandial hyperglycemia by inhibition of carbohydrate hydrolyzing enzyme such as alpha-amylase is one of the therapeutic approaches to treat Type 2 Diabetes. Alpha-amylase inhibitors from plants have been found to be effective in managing postprandial hyperglycemia. In continuation of our anti-diabetic activities of this plant, bioassay-guided fractionation and isolation using 0.1-1.0 mg/mL furnished djalonenol, a monoterpene diol with a significant 53.7% α-amylase inhibition (p<0.001) from the stem bark which was comparable to acarbose which gave a 54.9% inhibition. Spectral characterization using Infra-red, Gas Chromatogrphy-Mass spectrometry, 1D and 2D NMR of the isolated compound was done to elucidate the structure of the compound.

Keywords: alpha-amylase inhibitor, hyperglycemia, postprandial, diabetes

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Authors: Zhou Ziyi, Chen Qiuxiao, Wu Shuang

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Population diversification is very common in villages located in the developed coastal areas of China. Based on the analyses of the characteristics of the traditional rural society and its landscape, also in consideration of the diversified landscape demand due to the population diversification of the village, with the dual ideas of heritage and innovation, the ideas and methods of rural landscape design were explored by taking Duxuao Village in Zhejiang Province of China as an example.

Keywords: rural landscape, population diversification, landscape design, architecture

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Authors: Jyoti Singh, Ranju Bansal

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Fighting pain and inflammation is a common problem faced by physicians while dealing with a wide variety of diseases. Since ancient time nonsteroidal anti-inflammatory agents (NSAIDs) and opioids have been the cornerstone of treatment therapy, however, the usefulness of both these classes is limited due to severe side effects. NSAIDs, which are mainly used to treat mild to moderate inflammatory pain, induce gastric irritation and nephrotoxicity whereas opioids show an array of adverse reactions such as respiratory depression, sedation, and constipation. Moreover, repeated administration of these drugs induces tolerance to the analgesic effects and physical dependence. Further discovery of selective COX-2 inhibitors (coxibs) suggested safety without any ulcerogenic side effects; however, long-term use of these drugs resulted in kidney and hepatic toxicity along with an increased risk of secondary cardiovascular effects. The basic approaches towards inflammation and pain treatment are constantly changing, and researchers are continuously trying to develop safer and effective anti-inflammatory drug candidates for the treatment of different inflammatory conditions such as osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, psoriasis and multiple sclerosis. Synthetic 3(2H)-pyridazinones constitute an important scaffold for drug discovery. Structure-activity relationship studies on pyridazinones have shown that attachment of a lactam at N-2 of the pyridazinone ring through a methylene spacer results in significantly increased anti-inflammatory and analgesic properties of the derivatives. Further introduction of the heterocyclic ring at lactam nitrogen results in improvement of biological activities. Keeping in mind these SAR studies, a new series of compounds were synthesized as shown in scheme 1 and investigated for anti-inflammatory, analgesic, anti-platelet activities and docking studies. The structures of newly synthesized compounds have been established by various spectroscopic techniques. All the synthesized pyridazinone derivatives exhibited potent anti-inflammatory and analgesic activity. Homoveratryl substituted derivative was found to possess highest anti-inflammatory and analgesic activity displaying 73.60 % inhibition of edema at 40 mg/kg with no ulcerogenic activity when compared to standard drugs indomethacin. Moreover, 2-substituted-4-benzo[d][1,3]dioxole-6-phenylpyridazin-3(2H)-ones derivatives did not produce significant changes in bleeding time and emerged as safe agents. Molecular docking studies also illustrated good binding interactions at the active site of the cyclooxygenase-2 (hCox-2) enzyme.

Keywords: anti-inflammatory, analgesic, pyridazin-3(2H)-one, selective COX-2 inhibitors

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

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

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

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Authors: Othmane Bouferroum, Malika Boudraa

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In this study, a dual exponential model for CV formant transition is derived from locus theory of speech perception. Then, an algorithm for automatic vowel and consonant’s target formant frequency detection is developed and tested on real speech. The results show that vowels and consonants are detected through transitions rather than their small stable portions. Also, vowel reduction is clearly observed in our data. These results are confirmed by the observations made in perceptual experiments in the literature.

Keywords: acoustic invariance, coarticulation, formant transition, locus equation

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Authors: Mirna Febriani

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The use of stainless steel wires in the field of dentistry is widely used, especially for orthodontic and prosthodontic treatment using stainless steel wire. The oral cavity is the ideal environment for corrosion, which can be caused by saliva. Prevention of corrosion on stainless steel wires can be done by using an organic or non-organic corrosion inhibitor. One of the organic inhibitors that can be used to prevent corrosion is the leaves of breadfruit. The method used for this research using Atomic Absorption Spectrophotometric test. The results showed that the difference of chromium ion releases on soaking in saliva and breadfruit leaf extracts on days 1, 3, 7 and 14. Statically calculation with independent T-test with p < 0,05 showed the significant difference. The conclusion of this study shows that breadfruit leaf extract can inhibit the corrosion rate of stainless steel wires.

Keywords: chromium ion, stainless steel, artificial saliva, breadfruit leaf

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Authors: Justine Kiiza, Xu Jiafang

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The world’s demand for energy is increasing rapidly due to population growth and a reduction in shallow conventional oil and gas reservoirs, resorting to deeper and mostly unconventional reserves like shale oil and gas. Most shale formations contain a large amount of expansive sodium montmorillonite (Na-Mnt), due to high water adsorption, hydration, and when the drilling fluid filtrate enters the formation with high Mnt content, the wellbore wall can be unstable due to hydration and swelling, resulting to shrinkage, sticking, balling, time wasting etc., and well collapse in extreme cases causing complex downhole accidents and high well costs. Recently, polyamines like 1, 6 – hexane diamine (HEDA) have been used as typical drilling fluid shale inhibitors to minimize and/or cab clay mineral swelling and maintain the wellbore stability. However, their application is limited to shallow drilling due to their sensitivity to elevated temperature and pressure. Inorganic potassium salts i.e., KCl, have long been applied for restriction of shale formation hydration expansion in deep wells, but their use is limited due to toxicity. Understanding the adsorption behaviour of HEDA on Na-Mnt surfaces in present of organo-salts, organic K-salts e.g., HCO₂K - main component of organo-salt drilling fluid, is of great significance in explaining the inhibitory performance of polyamine inhibitors. Molecular dynamic simulations (MD) were applied to investigate the influence of HCO₂K and KCl on the adsorption mechanism of HEDA on the Na-Mnt surface. Simulation results showed that adsorption configurations of HEDA are mainly by terminal amine groups with a flat-lying alkyl hydrophobic chain. Its interaction with the clay surface decreased the H-bond number between H₂O-clay and neutralized the negative charge of the Mnt surface, thus weakening the surface hydration ability of Na-Mnt. The introduction of HCO₂K greatly improved inhibition ability, coordination of interlayer ions with H₂O as they were replaced by K+, and H₂O-HCOO- coordination reduced H₂O-Mnt interactions, mobility and transport capability of H₂O molecules were more decreased. While KCl showed little ability and also caused more hydration with time, HCO₂K can be used as an alternative for offshore drilling instead of toxic KCl, with a maximum concentration noted in this study as 1.65 wt%. This study provides a theoretical elucidation for the inhibition mechanism and adsorption characteristics of HEDA inhibitor on Na-Mnt surfaces in the presence of K+-salts and may provide more insight into the evaluation, selection, and molecular design of new clay-swelling high-performance WBDF systems used in oil and gas complex offshore drilling well sections.

Keywords: shale, hydration, inhibition, polyamines, organo-salts, simulation

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Authors: Patcharawalai Jaisamut, Kamonthip Wiwattanawongsa, Ruedeekorn Wiwattanapatapee

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Supersaturation of drugs in the gastrointestinal tract is one approach to increase the absorption of poorly water-soluble drugs. The stabilization of a supersaturated state was achieved by adding precipitation inhibitors that may act through a variety of mechanisms.In this study, the effect of the natural gums, acacia, gelatin, pectin and tragacanth on curcumin supersaturation in simulated gastric fluid (SGF) (pH 1.2), fasted state simulated gastric fluid (FaSSGF) (pH 1.6), and simulated intestinal fluid (SIF) (pH 6.8)was investigated. The results indicated that all natural gums significantly increased the curcum insolubility (about 1.2-6-fold)when compared to the absence of gum, and assisted in maintaining the supersaturated drug solution. Among the tested gums, pectin at 3% w/w was the best precipitation inhibitor with a significant increase in the degree of supersaturation about 3-fold in SGF, 2.4-fold in FaSSGF and 2-fold in SIF.

Keywords: curcumin, solubility, supersaturation, precipitation inhibitor

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Authors: Haniyeh Sameie

Abstract:

In the process of globalization, geographical boundaries gradually lose their importance, and ethnic, local, and regional cultures are integrated with each other and even marginalized. Globalization has many manifestations and aspects, including economic, political, social, etc., but this paper has focused on the cultural aspect of globalization. From this point of view, one of the important issues that have always been raised is the assimilation of diverse and plural cultures, which are gradually disappearing and destroyed in the onslaught of global culture and are dissolved in global culture. In the postmodern paradigm, the tools of the globalized world can be used to preserve and strengthen cultural diversity. For example, the Internet, as a globalization tool, can play an important role in preserving and recognizing local cultures. In today's world, the world nations and ethnic groups are trying to revive their specific and native cultures in different ways in opposition to the rising cultural assimilation and challenge the globalization of culture. One of the manifestations of these actions is addressing the issue of tourism and, specifically, eco-tourism, which is being developed in Iran as well as in other parts of the world, relying on the powerful tool of globalization, the Internet. Considering the significant growth of the ecotourism industry in Iran in recent years, this paper focuses on the role of the Internet in the development of ecotourism in Iran as one of the manifestations of tourism in recent decades and how to preserve and survive diverse local cultures and strengthen local communities against global culture through it. One of the major challenges in the development of communication technology in Iran in the last decade has been the debate over the necessity or non-necessity of access to high-speed Internet in the villages of Iran. Some believe that accessing the broadband internet in the villages may lead to the disappearance of local cultures and can facilitate the spread of western culture among villagers. On the other hand, the speed of expansion of ecotourism in Iran in the last ten years is owed to the development of the Internet in villages. In this regard, we pay attention to the dual role of the Internet in cultural assimilation and, at the same time, the platform that the online space has created for the growth and development of ecotourism accommodations as a source of stable income for local communities, focusing on the Iranian experience in the recent decade.

Keywords: tourism, globalization, internet, ecotourism in Iran, cultural assimilation

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Authors: Niv Papo

Abstract:

Characterizing the binding selectivity landscape of interacting proteins is crucial both for elucidating the underlying mechanisms of their interaction and for developing selective inhibitors. However, current mapping methods are laborious and cannot provide a sufficiently comprehensive description of the landscape. Here, we introduce a distinct and efficient strategy for comprehensively mapping the binding landscape of proteins using a combination of experimental multi-target selective library screening and in silico next-generation sequencing analysis. We map the binding landscape of a non-selective trypsin inhibitor, the amyloid protein precursor inhibitor (APPI), to each of four human serine proteases (kallikrein-6, mesotrypsin, and anionic and cationic trypsins). We then use this map to dissect and improve the affinity and selectivity of APPI variants toward each of the four proteases. Our strategy can be used as a platform for the development of a new generation of target-selective probes and therapeutic agents based on selective protein–protein interactions.

Keywords: drug design, directed evolution, protein engineering, protease inhibition.

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Authors: Jai Prakash Verma, Khushboo Verma

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In the present paper, a pair of Mond-Weir type non-differentiable multiobjective second-order programming problems, involving two kernel functions, where each of the objective functions contains support function, is formulated. We prove weak, strong and converse duality theorem for the second-order symmetric dual programs under η-pseudoinvexity conditions.

Keywords: non-differentiable multiobjective programming, second-order symmetric duality, efficiency, support function, eta-pseudoinvexity

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Authors: Najmeh Hoseini

Abstract:

Strokerecovery happens through neuroplasticity, which is highly influenced by the environment, including neuro-rehabilitation. Transcranial direct current stimulation (tDCS) may enhance recovery by modulating neuroplasticity. With tDCS, weak direct currents are applied noninvasively to modify excitability in the cortical areas under its electrodes. Combined with functional activities, this may facilitate motor recovery in neurologic disorders such as stroke. The purpose of this case study was to examine the effect of tDCS combined with 30 minutes of traditional physical therapy (PT)on arm function following a stroke. A 29-year-old male with chronic stroke involving the left middle cerebral artery territory went through the treatment protocol. Design The design included 5 weeks of treatment: 1 week of traditional PT, 2 weeks of sham tDCS combined with traditional PT, and 2 weeks of tDCS combined with traditional PT. PT included functional electrical stimulation (FES) of wrist extensors followed by task-specific functional training. Dual hemispheric tDCS with 1 mA intensity was applied on the sensorimotor cortices for the first 20 min of the treatment combined with FES. Assessments before and after each treatment block included Modified Ashworth Scale, ChedokeMcmaster Arm and Hand inventory, Action Research Arm Test (ARAT), and the Box and Blocks Test. Results showed reduced spasticity in elbow and wrist flexors only after tDCS combination weeks (+1 to 0). The patient demonstrated clinically meaningful improvements in gross motor and fine motor control over the duration of the study; however, components of the ARAT that require fine motor control improved the greatest during the experimental block. Average time improvement compared to baseline was26.29 s for tDCS combination weeks, 18.48 s for sham tDCS, and 6.83 for PT standard of care weeks. Combining dual hemispheric tDCS with the standard of care PT demonstrated improvements in hand dexterity greater than PT alone in this patient case.

Keywords: tDCS, stroke, case study, physical therapy

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Authors: Magno Enrique Mendoza Meza

Abstract:

This paper deals with the comparison of three control techniques: the hysteresis on-off control (HyOOC), the hybrid on-off control (HOOC) and the simple Structured Treatment Interruptions (sSTI). These techniques are applied to the mathematical model developed by Kirschner and Webb. To compare these techniques we use a cost functional that minimize the wild-type virus population and the mutant virus population, but the main objective is to minimize the systemic cost of treatment and maximize levels of healthy CD4+ T cells. HyOOC, HOOC, and sSTI are applied to the drug therapies using a reverse transcriptase and protease inhibitors; simulations show that these controls maintain the uninfected cells in a small, bounded neighborhood of a pre-specified level. The controller HyOOC and HOOC are designed by appropriate choice of virtual equilibrium points.

Keywords: virus dynamics, on-off control, hysteresis, multi-drug therapies

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Authors: Asli Faiza, Khamouli Saida

Abstract:

With the development of computer tools over the past 20 years. Molecular modeling and, more precisely, molecular docking has very quickly entered field of pharmaceutical research. EGFR enzyme involved in cancer disease.Our work consists of studying the inhibition of EGFR (1M17) with deferent inhibitors derived from quinazoline and quinoline by molecular docking. The values of ligands L148 and L177 are the best ligands for inhibit the activity of 1M17 since it forms a stable complex with this enzyme by better binding to the active site. The results obtained show that the ligands L148 and L177 give weak interactions with the active site residues EGFR (1M17), which stabilize the complexes formed of this ligands, which gives a better binding at the level of the active site, and an RMSD of L148 [1,9563 Å] and of L177 [ 1,2483 Å]. [1, 9563, 1.2483] Å

Keywords: docking, EGFR, quinazoline, quinoliène, MOE

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Authors: Ahmed A. Elshami, Stephanie Bonnet, Abdelhafid Khelidj

Abstract:

Corrosion inhibitors are widely used in concrete industry to reduce the corrosion rate of steel rebar which is present in contact with aggressive environments. The present work aims to using Zamzam water from well located within the Masjid al-Haram in Mecca, Saudi Arabia 20 m (66 ft) east of the Kaaba, the holiest place in Islam as corrosion inhibitor for steel in rain water and simulated acid rain. The effect of Zamzam water was investigated by electrochemical impedance spectroscopy (EIS) and Potentiodynamic polarization techniques in Department of Civil Engineering - IUT Saint-Nazaire, Nantes University, France. Zamzam water is considered to be one of the most important steel corrosion inhibitor which is frequently used in different industrial applications. Results showed that zamzam water gave a very good inhibition for steel corrosion in rain water and simulated acid rain.

Keywords: Zamzam water, corrosion inhibitor, rain water, simulated acid rain

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Authors: Deepika Bhaskar, Neena Wadehra, Megha Gulati, Aruna Narula, R. Vishnu, Gunjan Katyal

Abstract:

With drug resistance becoming widespread in Plasmodium falciparum infections, development of the alternative drugs is the desired strategy for prevention and cure of malaria. Three drug targets were selected to screen promising drug molecules from the GSK library of around 14000 molecules. Using an in silico structure-based drug designing approach, the differences in binding energies of the substrate and inhibitor were exploited between target sites of parasite and human to design a drug molecule against Plasmodium. The docking studies have shown several promising molecules from GSK library with more effective binding as compared to the already known inhibitors for the drug targets. Though stronger interaction has been shown by several molecules as compare to reference, few molecules have shown the potential as drug candidates though in vitro studies are required to validate the results.

Keywords: plasmodium, malaria, drug targets, in silico studies

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