Search results for: biological%20systems
Commenced in January 2007
Frequency: Monthly
Edition: International
Paper Count: 2316

Search results for: biological%20systems

936 Synthesis and Characterization of Some Novel Carbazole Schiff Bases (OLED)

Authors: Baki Cicek, Umit Calisir

Abstract:

Carbazoles have been replaced lots of studies from 1960's to present and also still continues. In 1987, the first diode device had been developed. Thanks to that study, light emitting devices have been investigated and developed and also have been used on commercial applications. Nowadays, OLED (Organic Light Emitting Diodes) technology is using on lots of electronic screen such as (mobile phone, computer monitors, televisions, etc.) Carbazoles were subject a lot of study as a semiconductor material. Although this technology is used commen and widely, it is still development stage. Metal complexes of these compounds are using at pigment dyes because of colored substances, polymer technology, medicine industry, agriculture area, preparing rocket fuel-oil, determine some of biological events, etc. Becides all of these to preparing of schiff base synthesis is going on intensely. In this study, some of novel carbazole schiff bases were synthesized starting from carbazole. For that purpose, firstly, carbazole was alkylated. After purification of N-substituted-carbazole was nitrated to sythesized 3-nitro-N-substituted and 3,6-dinitro-N-substituted carbazoles. At next step, nitro group/groups were reduced to amines. Purified with using a type of silica gel-column chromatography. At the last step of our study, with sythesized 3,6-diamino-N-substituted carbazoles and 3-amino-N-substituted carbazoles were reacted with aldehydes to condensation reactions. 3-(imino-p-hydroxybenzyl)-N-isobutyl -carbazole, 3-(imino-2,3,4-trimethoxybenzene)-N-butylcarbazole, 3-(imino-3,4-dihydroxybenzene)-N-octylcarbazole, 3-(imino-2,3-dihydroxybenzene)-N-octylkarbazole and 3,6-di(α-imino-β-naphthol) -N-hexylcarbazole compounds were synthesized. All of synthesized compounds were characterized with FT-IR, 1H-NMR, 13C-NMR, and LC-MS.

Keywords: carbazole, carbazol schiff base, condensation reactions, OLED

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935 The Metabolite Profiling of Fulvestrant-3 Boronic Acid under Biological Oxidation

Authors: Changde Zhang, Qiang Zhang, Shilong Zheng, Jiawang Liu, Shanchun Guo, Qiu Zhong, Guangdi Wang

Abstract:

Fulvestrant was approved by FDA to treat breast cancer as a selective estrogen receptor downregulator (SERD) with intramuscular injection administration. ZB716, a fulvestarnt-3 boronic acid, is an SERD with comparable anticancer effect to fulvestrant, but could produce good pharmacokinetic properties under oral administration with mice or rat models. To understand why ZB716 produced much better oral bioavailability, it was proposed that the boronic acid blocked the phase II direct biotransformation with the hydroxyl group on the 3 position of the aromatic ring on fulvestrant. In this study, ZB716 or fulvestrant was incubated with human liver microsome and oxidation cofactor NADPH in vitro. Their metabolites after oxidation were profiled with the Q-Exactive, a high-resolution mass spectrometer. The result showed that ZB716 blocked the forming of hydroxyl groups on its benzene ring except for the oxidation of C-B bond forming fulvestrant in its metabolites, and the concentration of fulvestrant with one more hydroxyl group found in the metabolites from incubation with fulvestrant was about 34 fold high as that formed from incubation with ZB716. Compared to fulvestrant, ZB716 is expected to be much difficult to be further bio-transformed into more hydrophilic compounds, to be difficult excreted out of blood system, and to have longer residence time in blood, which can lead to higher oral bioavailability. This study provided evidence to explain the high bioavailability of ZB716 after oral administration from the perspective of its difficulty of oxidation, a phase I biotransformation, on positions on its aromatic ring.

Keywords: biotransformation, fulvestrant, metabolite profiling, ZB716

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934 Immobilized Iron Oxide Nanoparticles for Stem Cell Reconstruction in Magnetic Particle Imaging

Authors: Kolja Them, Johannes Salamon, Harald Ittrich, Michael Kaul, Tobias Knopp

Abstract:

Superparamagnetic iron oxide nanoparticles (SPIONs) are nanoscale magnets which can be biologically functionalized for biomedical applications. Stem cell therapies to repair damaged tissue, magnetic fluid hyperthermia for cancer therapy and targeted drug delivery based on SPIONs are prominent examples where the visualization of a preferably low concentrated SPION distribution is essential. In 2005 a new method for tomographic SPION imaging has been introduced. The method named magnetic particle imaging (MPI) takes advantage of the nanoparticles magnetization change caused by an oscillating, external magnetic field and allows to directly image the time-dependent nanoparticle distribution. The SPION magnetization can be changed by the electron spin dynamics as well as by a mechanical rotation of the nanoparticle. In this work different calibration methods in MPI are investigated for image reconstruction of magnetically labeled stem cells. It is shown that a calibration using rotationally immobilized SPIONs provides a higher quality of stem cell images with fewer artifacts than a calibration using mobile SPIONs. The enhancement of the image quality and the reduction of artifacts enables the localization and identification of a smaller number of magnetically labeled stem cells. This is important for future medical applications where low concentrations of functionalized SPIONs interacting with biological matter have to be localized.

Keywords: biomedical imaging, iron oxide nanoparticles, magnetic particle imaging, stem cell imaging

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933 Planning Water Reservoirs as Complementary Habitats for Waterbirds

Authors: Tamar Trop, Ido Izhaki

Abstract:

Small natural freshwater bodies (SNFWBs), which are vital for many waterbird species, are considered endangered habitats due to their progressive loss and extensive degradation. While SNFWBs are becoming extinct, studies have indicated that many waterbird species may greatly benefit from various types of small artificial waterbodies (SAWBs), such as floodwater and treated water reservoirs. If designed and managed with care, SAWBs hold significant potential to serve as alternative or complementary habitats for birds, and thus mitigate the adverse effects of SNFWBs loss. Currently, most reservoirs are built as infrastructural facilities and designed according to engineering best practices and site-specific considerations, which do not include catering for waterbirds' needs. Furthermore, as things stand, there is still a lack of clear and comprehensive knowledge regarding the additional factors that should be considered in tackling the challenge of attracting waterbirds' to reservoirs, without compromising on the reservoirs' original functions. This study attempts to narrow this knowledge gap by performing a systematic review of the various factors (e.g., bird attributes; physical, structural, spatial, climatic, chemical, and biological characteristics of the waterbody; and anthropogenic activities) affecting the occurrence, abundance, richness, and diversity of waterbirds in SNFWBs. The methodical review provides a concise and relatively unbiased synthesis of the knowledge in the field, which can inform decision-making and practice regarding the planning, design, and management of reservoirs with birds in mind. Such knowledge is especially beneficial for arid and semiarid areas, where natural water sources are deteriorating and becoming extinct even faster due to climate change.

Keywords: artificial waterbodies, reservoirs, small waterbodies, waterbirds

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932 Experimental Study of the Dynamics of Sediments in Natural Channels in a Non-Stationary Flow Regime

Authors: Fourar Ali, Fourar Fatima Zohra

Abstract:

Knowledge of sediment characteristics is fundamental to understanding their sedimentary functioning: sedimentation, settlement, and erosion processes of cohesive sediments are controlled by complex interactions between physical, chemical, and biological factors. Sediment transport is of primary importance in river hydraulics and river engineering. Indeed, the displacement of sediments can lead to lasting modifications of the bed in terms of its elevation, slope and roughness. The protection of a bank, for example, is likely to initiate a local incision of the river bed, which, in turn, can lead to the subsidence of the bank. The flows in the natural environment occur in general with heterogeneous boundary conditions because of the distribution of the roughnesses of the fixed or mobile bottoms and of the important deformations of the free surface, especially for the flows with a weak draft considering the irregularity of the bottom. Bedforms significantly influence flow resistance. The arrangement of particles lining the bottom of the stream bed or experimental channel generates waveforms of different sizes that lead to changes in roughness and consequently spatial variability in the turbulent characteristics of the flow. The study which is focused on the laws of friction in alluvial beds, aims to analyze the characteristics of flows and materials constituting the natural channels. Experimental results were obtained by simulating these flows on a rough bottom in an experimental channel at the Hydraulics Laboratory of the University of Batna 2. The system of equations governing the problem is solved using the program named: CLIPPER.5 and ACP.

Keywords: free surface flow, heterogeneous sand, moving bottom bed, friction coefficient, bottom roughness

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931 A Modular and Reusable Bond Graph Model of Epithelial Transport in the Proximal Convoluted Tubule

Authors: Leyla Noroozbabaee, David Nickerson

Abstract:

We introduce a modular, consistent, reusable bond graph model of the renal nephron’s proximal convoluted tubule (PCT), which can reproduce biological behaviour. In this work, we focus on ion and volume transport in the proximal convoluted tubule of the renal nephron. Modelling complex systems requires complex modelling problems to be broken down into manageable pieces. This can be enabled by developing models of subsystems that are subsequently coupled hierarchically. Because they are based on a graph structure. In the current work, we define two modular subsystems: the resistive module representing the membrane and the capacitive module representing solution compartments. Each module is analyzed based on thermodynamic processes, and all the subsystems are reintegrated into circuit theory in network thermodynamics. The epithelial transport system we introduce in the current study consists of five transport membranes and four solution compartments. Coupled dissipations in the system occur in the membrane subsystems and coupled free-energy increasing, or decreasing processes appear in solution compartment subsystems. These structural subsystems also consist of elementary thermodynamic processes: dissipations, free-energy change, and power conversions. We provide free and open access to the Python implementation to ensure our model is accessible, enabling the reader to explore the model through setting their simulations and reproducibility tests.

Keywords: Bond Graph, Epithelial Transport, Water Transport, Mathematical Modeling

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930 The Role of Micro-Ribonucleic Acid-182 and Micro-Ribonucleic Acid-214 in Cisplatin Resistance of Triple-Negative Breast Cancer Cells

Authors: Bahadir Batar, Elif Serdal, Berna Erdal, Hasan Ogul

Abstract:

Micro-ribonucleic acids (miRNAs) are small short non-coding ribonucleic acid molecules about 22 nucleotides long. miRNAs play a key role in response to chemotherapeutic agents. WW domain-containing oxidoreductase (WWOX) gene encodes a tumor suppressor protein. Loss or reduction of Wwox protein is observed in many breast cancer cases. WWOX protein deficiency is increased in triple-negative breast cancer (TNBC). TNBC is a heterogeneous, highly aggressive, and difficult to treat tumor type. WWOX loss contributes to resistance to cisplatin therapy in patients with TNBC. Here, the aim of the study was to investigate the potential role of miRNAs in cisplatin therapy resistance of WWOX-deficient TNBC cells. This was a cell culture study. miRNA expression profiling was analyzed by LightCycler 480 system. miRNA Set Enrichment Analysis tool was used to integrate experimental data with literature-based biological knowledge to infer a new hypothesis. Increased miR-182 and decreased miR-214 were significantly correlated with cisplatin resistance in WWOX-deficient TNBC cells. miR-182 and miR-214 may involve in cisplatin resistance of WWOX-deficient TNBC cells by deregulating the DNA repair, apoptosis, or protein kinase B signaling pathways. These data highlight the mechanism by which WWOX regulates cisplatin resistance of TNBC and the potential use of WWOX as a predictor biomarker for cisplatin resistance.

Keywords: cisplatin, microRNA, triple-negative breast cancer, WWOX

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929 Investigating the Formation of Nano-Hydroxyapatite on a Biocompatible and Antibacterial Cu/Mg-Substituted Bioglass

Authors: Elhamalsadat Ghaffari, Moghan Amirhosseinian, Amir Khaleghipour

Abstract:

Multifunctional bioactive glasses (BGs) are designed with a focus on the provision of bactericidal and biological properties desired for angiogenesis, osteogenesis, and ultimately potential applications in bone tissue engineering. To achieve these, six sol-gel copper/magnesium substituted derivatives of 58S-BG, i.e. a mol% series of 60SiO2-4P2O5-5CuO-(31-x) CaO/xMgO (where x=0, 1, 3, 5, 8, and 10), were synthesized. Afterwards, the effect of MgO/CaO substitution on the in vitro formation of nano-hydroxyapatite (HA), osteoblast-like cell responses and BGs antibacterial performance were studied. During the BGs synthesis, the elimination of nitrates was achieved at 700 °C that prevented the BGs crystallization and stabilized the obtained dried gels. The structural and morphological evaluations were performed with X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), and scanning electron microscopy (SEM). These characterizations revealed that Cu-substituted 58S-BG consisting of 5 mol% MgO (BG-5/5) slightly had retarded the formation of HA. In addition, Cu-substituted 58S-BGs consisting 8 mol% and 10 mol% MgO (BG-5/8 and BG-5/10) displayed lower bioactivity probably due to the lower ion release rate of Ca–Si into the simulated body fluid (SBF). The determination of 3-(4, 5 dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) and alkaline phosphate (ALP) activities proved that the highest values of both differentiation and proliferation of MC3T3-E1 cells can be obtained from a 5 mol% MgO substituted BG, while the over addition of MgO (8 mol% and 10 mol%) decreased the bioactivity. Furthermore, these novel Cu/Mg-substituted 58S-BGs displayed antibacterial effect against methicillin-resistant Staphylococcus aureus bacteria. Taken together, the results suggest the equally-substituted BG-5/5 (i.e. the one consists of 5 mol% of both CuO and MgO) as a promising candidate for bone tissue engineering, among all newly designed BGs in this work, owing to its desirable cell proliferation, ALP activity and antibacterial properties.

Keywords: apatite, bioactivity, biomedical applications, sol-gel processes

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928 Inferring the Ecological Quality of Seagrass Beds from Using Composition and Configuration Indices

Authors: Fabrice Houngnandan, Celia Fery, Thomas Bockel, Julie Deter

Abstract:

Getting water cleaner and stopping global biodiversity loss requires indices to measure changes and evaluate the achievement of objectives. The endemic and protected seagrass species Posidonia oceanica is a biological indicator used to monitor the ecological quality of marine Mediterranean waters. One ecosystem index (EBQI), two biotic indices (PREI, Bipo), and several landscape indices, which measure the composition and configuration of the P. oceanica seagrass at the population scale have been developed. While the formers are measured at monitoring sites, the landscape indices can be calculated for the entire seabed covered by this ecosystem. This present work aims to search on the link between these indices and the best scale to be used in order to maximize this link. We used data collected between 2014 to 2019 along the French Mediterranean coastline to calculate EBQI, PREI, and Bipo at 100 sites. From the P. oceanica seagrass distribution map, configuration and composition indices around these different sites in 6 different grid sizes (100 m x 100 to 1000 m x 1000 m) were determined. Correlation analyses were first used to find out the grid size presenting the strongest and most significant link between the different types of indices. Finally, several models were compared basis on various metrics to identify the one that best explains the nature of the link between these indices. Our results showed a strong and significant link between biotic indices and the best correlations between biotic and landscape indices within the 600 m x 600 m grid cells. These results showed that the use of landscape indices is possible to monitor the health of seagrass beds at a large scale.

Keywords: ecological indicators, decline, conservation, submerged aquatic vegetation

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927 Upconversion Nanomaterials for Applications in Life Sciences and Medicine

Authors: Yong Zhang

Abstract:

Light has proven to be useful in a wide range of biomedical applications such as fluorescence imaging, photoacoustic imaging, optogenetics, photodynamic therapy, photothermal therapy, and light controlled drug/gene delivery. Taking photodynamic therapy (PDT) as an example, PDT has been proven clinically effective in early lung cancer, bladder cancer, head, and neck cancer and is the primary treatment for skin cancer as well. However, clinical use of PDT is severely constrained by the low penetration depth of visible light through thick tissue, limiting its use to target regions only a few millimeters deep. One way to enhance the range is to use invisible near-infrared (NIR) light within the optical window (700–1100nm) for biological tissues, extending the depth up to 1cm with no observable damage to the intervening tissue. We have demonstrated use of NIR-to-visible upconversion fluorescent nanoparticles (UCNPs), emitting visible fluorescence when excited by a NIR light at 980nm, as a nanotransducer for PDT to convert deep tissue-penetrating NIR light to visible light suitable for activating photosensitizers. The unique optical properties of UCNPs enable the upconversion wavelength to be tuned and matched to the activation absorption wavelength of the photosensitizer. At depths beyond 1cm, however, tissue remains inaccessible to light even within the NIR window, and this critical depth limitation renders existing phototherapy ineffective against most deep-seated cancers. We have demonstrated some new treatment modalities for deep-seated cancers based on UCNP hydrogel implants and miniaturized, wirelessly powered optoelectronic devices for light delivery to deep tissues.

Keywords: upconversion, fluorescent, nanoparticle, bioimaging, photodynamic therapy

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926 Bifunctional Electrospun Fibers Based on Poly(Lactic Acid)/Calcium Oxide Nanocomposites as a Potential Scaffold for Bone Tissue Engineering

Authors: Daniel Canales, Fabián Alvarez, Pablo Varela, Marcela Saavedra, Claudio García, Paula Zapata

Abstract:

Calcium oxide nanoparticles (n-CaO) ca. 8 nm were obtained from eggshell waste. The n-CaO was incorporated into Poly(lactic acid) PLA matrix in 10 and 20 wt.% of filler content by electrospinning process to obtain PLA/n-CaO nanocomposite fibers as a potential use in scaffold for bone tissue regeneration. The fibers morphology and diameter were homogeneity, the PLA had a diameter of 2.2 ± 0.8 µm and, with the nanoparticles incorporation (20wt.%), reached ca. 2.9 ± 0.9 µm. The PLA/n-CaO nanocomposites fibers showed in vitro bioactivity, capable of inducing the precipitation of hydroxyapatite (HA) layer in the fiber surface after 7 days in Simulated Body Solution (SBF). The biocidal and biological properties of PLA/n-Cao with 20 wt.% were evaluated, showing a 30% reduction in bacterial viability against S. aureus and 11% for E. coli after 6 hours of bacterial suspensions exposure. Furthermore, the fibers did not show a cytotoxic effect on the bone marrow ST-2 cell line, permitting the cell adhesion and proliferation in Roswell Park Memorial Institute medium (RPMI). The PLA/n-CaO with 20 wt.% of nanoparticles showed a higher capacity to promote the osteogenic differentiation, significantly increasing the alkaline phosphatase (ALP) expression after 7 days compared to PLA and cell control. The in vivo analysis corroborated the biocompatibility of scaffolds prepared, the presence of n-CaO in PLA reduced the formation of fibrous encapsulation of the material improve the healing process.

Keywords: electrospun scaffolds, PLA based nanocomposites, calcium oxide nanoparticles, bioactive materials, tissue engineering

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925 Enzyme Immobilization: A Strategy to Overcome Enzyme Limitations and Expand Their Applications

Authors: Charline Monnier, Rudolf Andrys, Irene Castellino, Lucie Zemanova

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Due to their inherent sustainability and compatibility with green chemistry principles, enzymes are attracting increasing attention for various applications like bioremediation or biocatalysis. These natural catalysts boast remarkable substrate specificity and operate under mild biological conditions. However, their intrinsic limitations, such as instability at high temperatures or in organic solvents, impede their wider applicability. Enzyme immobilization on supportive matrices emerges as a promising strategy to address these challenges. This approach not only facilitates enzyme reusability but also offers the potential to modulate their stability, activity, and selectivity. The present study investigates the immobilization and application of two distinct groups of hydrolases on supportive matrices: PETases, naturally capable of PolyEthylene Terephthalate (PET) degradation, and cholinesterases (ChEs), key enzymes in neurotransmitter regulation. All tested enzymes will be immobilized on porous and non-porous particles using both covalent and non-covalent methods. Additionally, the stability of PETases and cholinesterases will be explored, followed by exposure to denaturing conditions to assess their resilience under harsh conditions. Furthermore, due to the exceptional catalytic efficiency and selectivity, their biocatalytic efficiency will be tested using xenobiotic substrates, aiming to establish them as replacements for conventional chemical catalysts in environmentally friendly processes. By exploiting the power of enzyme immobilization, this research strives to unlock the full potential of these biocatalysts for sustainable and efficient technological advancements.

Keywords: biocatalysis, bioremediation, enzyme efficiency, enzyme immobilization, green chemistry

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924 Health and Safety of Red Cross Workers in Long-Term Homes during Early Days of the COVID-19 Pandemic: A Human Performance Perspective

Authors: Douglas J. Kube

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At the beginning of the COVID-19 pandemic, the Canadian Red Cross deployed workers into long-term care homes across Canada to support our most vulnerable citizens. It began by recruiting and training small teams of workers to provide non-clinical services for facilities in outbreak. Deployed workers were trained on an approach based on successful Red Cross deployments used with Ebola in which zones were established, levels of protection used, and strict protocols followed to prevent exposure. This paper addresses aspects of human performance through a safety culture lens. The Red Cross deployments highlight valuable insights and are an excellent case study in the principles of human performance and organizational culture. This paper looks at human performance principles, including human fallibility, predictability of error-likely situations, avoiding events by understanding reasons mistakes occur, and the influence on behaviour by organizational factors. This study demonstrates how the Red Cross’s organizational culture and work design positively influenced performance to protect workers and residents/clients. Lastly, this paper shares lessons that can be applied in many workplaces to improve worker health and safety and safety culture. This critical examination is based on the author’s experience as a Senior Occupational Health and Safety Advisor with the Red Cross during the pandemic as part of the team responsible for developing and implementing biological safety practices in long-term care deployments.

Keywords: COVID, human performance, organizational culture, work design

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923 Evaluation of Newly Synthesized Steroid Derivatives Using In silico Molecular Descriptors and Chemometric Techniques

Authors: Milica Ž. Karadžić, Lidija R. Jevrić, Sanja Podunavac-Kuzmanović, Strahinja Z. Kovačević, Anamarija I. Mandić, Katarina Penov-Gaši, Andrea R. Nikolić, Aleksandar M. Oklješa

Abstract:

This study considered selection of the in silico molecular descriptors and the models for newly synthesized steroid derivatives description and their characterization using chemometric techniques. Multiple linear regression (MLR) models were established and gave the best molecular descriptors for quantitative structure-retention relationship (QSRR) modeling of the retention of the investigated molecules. MLR models were without multicollinearity among the selected molecular descriptors according to the variance inflation factor (VIF) values. Used molecular descriptors were ranked using generalized pair correlation method (GPCM). In this method, the significant difference between independent variables can be noticed regardless almost equal correlation between dependent variable. Generated MLR models were statistically and cross-validated and the best models were kept. Models were ranked using sum of ranking differences (SRD) method. According to this method, the most consistent QSRR model can be found and similarity or dissimilarity between the models could be noticed. In this study, SRD was performed using average values of experimentally observed data as a golden standard. Chemometric analysis was conducted in order to characterize newly synthesized steroid derivatives for further investigation regarding their potential biological activity and further synthesis. This article is based upon work from COST Action (CM1105), supported by COST (European Cooperation in Science and Technology).

Keywords: generalized pair correlation method, molecular descriptors, regression analysis, steroids, sum of ranking differences

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922 Dual Mode Mobile Based Detection of Endogenous Hydrogen Sulfide for Determination of Live and Antibiotic Resistant Bacteria

Authors: Shashank Gahlaut, Chandrashekhar Sharan, J. P. Singh

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Increasing incidence of antibiotic-resistant bacteria is a big concern for the treatment of pathogenic diseases. The effect of treatment of patients with antibiotics often leads to the evolution of antibiotic resistance in the pathogens. The detection of antibiotic or antimicrobial resistant bacteria (microbes) is quite essential as it is becoming one of the big threats globally. Here we propose a novel technique to tackle this problem. We are taking a step forward to prevent the infections and diseases due to drug resistant microbes. This detection is based on some unique features of silver (a noble metal) nanorods (AgNRs) which are fabricated by a physical deposition method called thermal glancing angle deposition (GLAD). Silver nanorods are found to be highly sensitive and selective for hydrogen sulfide (H2S) gas. Color and water wetting (contact angle) of AgNRs are two parameters what are effected in the presence of this gas. H₂S is one of the major gaseous products evolved in the bacterial metabolic process. It is also known as gasotransmitter that transmits some biological singles in living systems. Nitric Oxide (NO) and Carbon mono oxide (CO) are two another members of this family. Orlowski (1895) observed the emission of H₂S by the bacteria for the first time. Most of the microorganism produce these gases. Here we are focusing on H₂S gas evolution to determine live/dead and antibiotic-resistant bacteria. AgNRs array has been used for the detection of H₂S from micro-organisms. A mobile app is also developed to make it easy, portable, user-friendly, and cost-effective.

Keywords: antibiotic resistance, hydrogen sulfide, live and dead bacteria, mobile app

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921 A Literature Review: The Anti-Obesity Effect of Epigallocathecin-3-Gallate of Camellia sinensis (Green Tea) Extraction as a Potential Adjuvant Therapy for Management Obesity

Authors: Nunuy Nuraeni, Vera Amalia Lestari, Atri Laranova, Viena Nissa Mien Fadhillah, Mutia, Muhammad Ikhlas Abdian Putra

Abstract:

Introduction: Obesity is a common disease with high prevalence especially in developing countries including Indonesia. The obesitygenic lifestyle such as excessive intake of food, sedentary lifestyle is the major environmental etiologies of obesity. Obesity is also as one of burden disease with high morbidity due to its complication, such as diabetes mellitus and hypertension. The objective of this literature review is to know how the Epigallocathecin-3-Gallate of Green tea or Camellia sinensis effect as anti-obesity agent and reduce the complication of obesity. Material and Methods: This study based on the secondary data analysis complemented by primary data collection from several journal and textbook. We identified the effect of Epigallocathecin-3-Gallate of Green tea or Camellia sinensis as adjuvant therapy for management obesity and to prevent the complications of obesity. Results: Based on the result, Green tea or Camellia sinensis contain Epigallocathecin-3-Gallate (EGCG) that has anti-obesity effect such as induce apoptosis, inhibit adipogenesis, increasing lipolytic activity, increasing fat oxidation and thermogenesis. Discussion: EGCG are naturally distributed in green tea, that contains a biological activity that has a potential effect to treat obesity. Conclusion: EGCG are capable to treat obesity. By consuming EGCG can prevent obesity in normal health person and prevent complication in patient with obesity.

Keywords: adjuvant therapy, anti-obesity effect, complication, epigallocathecin-3-gallate, obesity

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920 Bio-Guided of Active New Alkaloids from Alstonia Brassi Toxicity Antitumour Activity in Silico and Molecular Modeling

Authors: Mesbah Khaled, Bouraoui Ouissal, Benkiniouar Rachid, Belkhiri Lotfi

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Alstonia, which are tropical plants with a wide geographical distribution, have been divided into different sections by different authors based on previous studies of several species within the genus. Monachino divides Alstonia into 5 sections, while Pichon divides it into 3 sections. Several plants belonging to this genus, such as Alstonia brassii, have been used in traditional folk medicine to treat ailments such as fever, malaria and dysentery]. Previous studies focusing on the chemical composition of these plants have successfully identified indol alkaloids with cytotoxic, anti-diabetic and anti-inflammatory properties. The newly discovered monomers are structurally similar to the backbones of picralin, affinisin and macrolin. On the other hand, all recently isolated dimeric compounds have a macrolin moiety. In this study, a computational analysis was performed on a series of novel molecules, including both monomeric and dimeric compounds with different structural frameworks. This investigation represents the first computational study of these molecules using an in silico approach incorporating 2D-QSAR data. The analysis involved various computational techniques, including 2D-QSAR modelling, molecular docking studies and subsequent validation by molecular dynamics simulation and assessment of ADMET properties. The chemical composition was identified by 1D and 2D NMR. Eight new alkaloids were isolated, 5 monomers and 3 dimers. In this section, we focus on the biological activity of 4 new alkaloids belonging to two different skeletons, the affinisine skeleton.

Keywords: affinisine, talcarpine, macroline, cytotoxicity, alkaloids

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919 Short-Term versus Long-Term Effect of Waterpipe Smoking Exposure on Cardiovascular Biomarkers in Mice

Authors: Abeer Rababa'h, Ragad Bsoul, Mohammad Alkhatatbeh, Karem Alzoubi

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Introduction: Tobacco use is one of the main risk factors to cardiovascular diseases (CVD) and atherosclerosis in particular. WPS contains several toxic materials such as: nicotine, carcinogens, tar, carbon monoxide and heavy metals. Thus, WPS is considered to be as one of the toxic environmental factors that should be investigated intensively. Therefore, the aim of this study is to investigate the effect of WPS on several cardiovascular biological markers that may cause atherosclerosis in mice. The study also conducted to study the temporal effects of WPS on the atherosclerotic biomarkers upon short (2 weeks) and long-term (8 weeks) exposures. Methods: mice were exposed to WPS and heart homogenates were analyzed to elucidate the effects of WPS on matrix metalloproteinase (MMPs), endothelin-1 (ET-1) and, myeloperoxidase (MPO). Following protein estimation, enzyme-linked immunosorbent assays were done to measure the levels of MMPs (isoforms 1, 3, and 9), MPO, and ET-1 protein expressions. Results: our data showed that acute exposure to WPS significantly enhances the levels of MMP-3, MMP- 9, and MPO expressions (p < 0.05) compared to their corresponding control. However, the body was capable to normalize the level of expressions for such parameters following continuous exposure for 8 weeks (p > 0.05). Additionally, we showed that the level of ET-1 expression was significantly higher upon chronic exposure to WPS compared to both control and acute exposure groups (p < 0.05). Conclusion: Waterpipe exposure has a significant negative effect on atherosclerosis and the enhancement of the atherosclerotic biomarkers expression (MMP-3 and 9, MPO, and ET-1) might represent an early scavenger of compensatory efforts to maintain cardiac function after WP exposure.

Keywords: atherosclerotic biomarkers, cardiovascular disease, matrix metalloproteinase, waterpipe

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918 Preservation of Sensitive Biological Products: An Insight into Conventional and Upcoming Drying Techniques

Authors: Jannika Dombrowski, Sabine Ambros, Ulrich Kulozik

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Several drying techniques are used to preserve sensitive substances such as probiotic lactic acid bacteria. With the aim to better understand differences between these processes, this work gives new insights into structural variations resulting from different preservation methods and their impact on product quality and storage stability. Industrially established methods (freeze drying, spray drying) were compared to upcoming vacuum, microwave-freeze, and microwave-vacuum drying. For freeze and microwave-freeze dried samples, survival and activity maintained 100%, whereas vacuum and microwave-vacuum dried cultures achieved 30-40% survival. Spray drying yielded in lowest viability. The results are directly related to temperature and oxygen content during drying. Interestingly, most storage stable products resulted from vacuum and microwave-vacuum drying due to denser product structures as determined by helium pycnometry and SEM images. Further, lower water adsorption velocities were responsible for lower inactivation rates. Concluding, resulting product structures as well as survival rates and storage stability mainly depend on the type of water removal instead of energy input. Microwave energy compared to conductive heating did not lead to significant differences regarding the examined factors. Correlations could be proven for three investigated microbial strains. The presentation will be completed by an overview on the energy efficiency of the presented methods.

Keywords: drying techniques, energy efficiency, lactic acid bacteria, probiotics, survival rates, structure characterization

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917 Determination of Antioxidant Activity in Raphanus raphanistrum L.

Authors: Esma Hande Alıcı, Gülnur Arabacı

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Antioxidants are compounds or systems that can safely interact with free radicals and terminate the chain reaction before vital molecules are damaged. The anti-oxidative effectiveness of these compounds depends on their chemical characteristics and physical location within a food (proximity to membrane phospholipids, emulsion interfaces, or in the aqueous phase). Antioxidants (e.g., flavonoids, phenolic acids, tannins, vitamin C, vitamin E) have diverse biological properties, such as antiinflammatory, anti-carcinogenic and anti-atherosclerotic effects, reduce the incidence of coronary diseases and contribute to the maintenance of gut health by the modulation of the gut microbial balance. Plants are excellent sources of antioxidants especially with their high content of phenolic compounds. Raphanus raphanistrum L., the wild radish, is a flowering plant in the family Brassicaceae. It grows in Asia and Mediterranean region. It has been introduced into most parts of the world. It spreads rapidly, and is often found growing on roadsides or in other places where the ground has been disturbed. It is an edible plant, in Turkey its fresh aerial parts are mostly consumed as a salad with olive oil and lemon juice after boiled. The leaves of the plant are also used as anti-rheumatic in traditional medicine. In this study, we determined the antioxidant capacity of two different solvent fractions (methanol and ethyl acetate) obtained from Raphanus raphanistrum L. plant leaves. Antioxidant capacity of the plant was introduced by using three different methods: DPPH radical scavenging activity, CUPRAC (Cupric Ion Reducing Antioxidant Capacity) activity and Reducing power activity.

Keywords: antioxidant activity, antioxidant capacity, Raphanis raphanistrum L., wild radish

Procedia PDF Downloads 275
916 Surface Modified Quantum Dots for Nanophotonics, Stereolithography and Hybrid Systems for Biomedical Studies

Authors: Redouane Krini, Lutz Nuhn, Hicham El Mard Cheol Woo Ha, Yoondeok Han, Kwang-Sup Lee, Dong-Yol Yang, Jinsoo Joo, Rudolf Zentel

Abstract:

To use Quantum Dots (QDs) in the two photon initiated polymerization technique (TPIP) for 3D patternings, QDs were modified on the surface with photosensitive end groups which are able to undergo a photopolymerization. We were able to fabricate fluorescent 3D lattice structures using photopatternable QDs by TPIP for photonic devices such as photonic crystals and metamaterials. The QDs in different diameter have different emission colors and through mixing of RGB QDs white light fluorescent from the polymeric structures has been created. Metamaterials are capable for unique interaction with the electrical and magnetic components of the electromagnetic radiation and for manipulating light it is crucial to have a negative refractive index. In combination with QDs via TPIP technique polymeric structures can be designed with properties which cannot be found in nature. This makes these artificial materials gaining a huge importance for real-life applications in photonic and optoelectronic. Understanding of interactions between nanoparticles and biological systems is of a huge interest in the biomedical research field. We developed a synthetic strategy of polymer functionalized nanoparticles for biomedical studies to obtain hybrid systems of QDs and copolymers with a strong binding network in an inner shell and which can be modified in the end through their poly(ethylene glycol) functionalized outer shell. These hybrid systems can be used as models for investigation of cell penetration and drug delivery by using measurements combination between CryoTEM and fluorescence studies.

Keywords: biomedical study models, lithography, photo induced polymerization, quantum dots

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915 Assessment of Phytoremediation of Pb-Anthracene Co-Contaminated Soils Using Vetiveira zizanioides, Heianthus annuus L., Zea mays and Glycine max

Authors: O. U. Nwosu, C. O. Osuagwu, N. Nnawugwu, C. T. Amanze

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Phytoremediation is a green and sustainable approach to decontaminate and restore contaminated sites while maintaining the biological activity and physical structure of soils. A pot experiment was conducted for a period of 70 days to evaluate the remediation potentials of Vetiveira zizanioides, Heianthus annuus L., Zea mays, and Glycine max in concurrent removal of anthracene and Pb in co-contaminated soil. Sandy loam soils were polluted with Pb chloride salt and anthracene at three different levels (50mg/kg of Pb, 100mg/kg of Pb, and 100mg/kg of Pb+100mg/kg of anthracene) and laid out in a completely randomized design with three replicates. Shoot dry matter weight was significantly reduced (p≤0.05) in comparison to control treatments by 33%, 32%, 40%, and 6.7% when exposed to 100mg kg⁻¹ of Pb, respectively in G.max, H.annuus, Z.mays, and vetiver. There was 42%, 41%, 48%, and 7.1% growth inhibition of shoot dry matter weight of G.max, H.annuus, Z.mays, and vetiver relative to control treatments when 100 mg Pb kg⁻¹ was mixed with 100 mgkg⁻¹ anthracene. Root and shoot metal concentration in G.max, H.annuus, Z.mays, and vetiver increased with increasing concentration of Pb. Translocation factor (TF < 1) obtained for G.max, Z.mays, and vetiver suggests that these plant species predominantly retain Pb in the root portion, while the TF value (TF≥1) obtained for H.annuus suggests that it predominantly retains Pb in the shoot portion. The extractable anthracene decreased significantly (p ≤ 0.05) in soil planted with G.max, H.annuus, Z.mays, and vetiver, as well as in pots without plants. This accounted for 53% to 71% of anthracene dissipation in planted soil and 40% dissipation in unplanted soil. This result suggested that the plant species used are a promising candidate for phytoremediation.

Keywords: phytoremediation, heavy metals, polyaromatic hydrocarbon, co-contaminated soil

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914 Seroprevalence and Associated Factors of Hepatitis B and Hepatitis C Viral Infections Among Prisoners in Tigray, Northern Ethiopia

Authors: Belaynesh Tsegay, Teklay Gebrecherkos, Atsebaha Gebrekidan Kahsay, Mahmud Abdulkader

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Background: Hepatitis B and C viruses are important health and socioeconomic problem across the globe, with a remarkable number of diseases and deaths in sub-Saharan African countries. The burden of hepatitis is unknown in the prison settings of Tigray. Therefore, we aimed to describe the seroprevalence and associated factors of hepatitis B and C viruses among prisoners in Tigray, Ethiopia. Methods: A cross-sectional study was carried out from February 2020 to May 2020 at the prison facilities of Tigray. Demographics and associated factors were collected from 315 prisoners prospectively. Five milliliters of blood were collected and tested using rapid tests kits of HBsAg (Zhejiang orient Gene Biotech Co., Ltd., China) and HCV antibodies (Volkan Kozmetik Sanayi Ve Ticaret Ltd. STI, Turkey). Positive samples were confirmed using ELISA (Beijing Wantai Biological Pharmacy Enterprise Co. Ltd). Data were analyzed using the SPSS version 20, and p<0.05 was considered statistically significant. Results: The overall seroprevalence of HBV and HCV were 25 (7.9%) and 1 (0.3%), respectively. The majority of hepatitis B viral infections were identified from the age groups of 18–25 years (10.7%) and unmarried prisoners (11.8%). Prisoners greater than 100 per cell (AOR=3.95, 95% CI=1.15–13.6, p=0.029) and with a history of alcohol consumption (AOR=3.01, 95% CI=1.17–7.74, p=0.022) were significantly associated with HBV infections. Conclusion: The seroprevalence of HBV among prisoners was nearly high or borderline, with a very low HCV prevalence. HBV was most prevalent among young adults, those housed with a large number of prisoners per cell, and those who had a history of alcohol consumption. This study recommends that there should be prison-focused intervention, including regular health education, with the emphasis on the mode of transmission and introducing HBV screening policy for prisoners, especially when they enter the prison.

Keywords: seroprevalence, HBV, HCV, prisoners, tigray

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913 Biodegradation of Direct Red 23 by Bacterial Consortium Isolated from Dye Contaminated Soil Using Sequential Air-lift Bioreactor

Authors: Lata Kumari Dhanesh Tiwary, Pradeep Kumar Mishra

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The effluent coming from various industries such as textile, carpet, food, pharmaceutical and many other industries is big challenge due to its recalcitrant and xenobiotiocs in nature. Recently, biodegradation of dye wastewater through biological means was widely used due to eco-friendly and cost effective with the higher percentage of removal of dye from wastewater. The present study deals with the biodegradation and decolourization of Direct Red 23 dye using indigenously isolated bacterial consortium. The bacterial consortium was isolated from soil sample from dye contaminated site near a cluster of Carpet industries of Bhadohi, Uttar Pradesh, India. The bacterial strain formed consortia were identified and characterized by morphological, biochemical and 16S rRNA gene sequence analysis. The bacterial strain mainly Staphylococcus saprophyticus strain BHUSS X3 (KJ439576), Microbacterium sp. BHUMSp X4 (KJ740222) and Staphylococcus saprophyticus strain BHUSS X5 (KJ439576) were used as consortia for further studies of dye decolorization. Experimental investigations were made in a Sequencing Air- lift bioreactor using the synthetic solution of Direct Red 23 dye by optimizing various parameters for efficient degradation of dye. The effect of several operating parameters such as flow rate, pH, temperature, initial dye concentration and inoculums size on removal of dye was investigated. The efficiency of isolated bacterial consortia from dye contaminated area in Sequencing Air- lift Bioreactor with different concentration of dye between 100-1200 mg/l at different hydraulic rate (HRTs) 26h and 10h. The maximum percentage of dye decolourization 98% was achieved when operated at HRT of 26h. The percentage of decolourization of dye was confirmed by using UV-Vis spectrophotometer and HPLC.

Keywords: carpet industry, bacterial consortia, sequencing air-lift bioreactor

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912 Mechanical Properties of Young and Senescence Fibroblast Cells Using Passive Microrheology

Authors: Samira Khalaji, , Fenneke Klein Jan, Kay-E. Gottschalk, Eugenia Makrantonaki, Karin Scharffetter-Kochanek

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Biological aging is a multi-dimensional process that takes place over a whole range of scales from the nanoscopic alterations within individual cells, over transformations in tissues and organs and to changes of the whole organism. On the single cell level, aging involves mutation of genes, differences in gene expression levels as well as altered posttranslational modifications of proteins. A variety of proteins is affected, including proteins of the cell cytoskeleton and migration machinery. Previous work quantified the expression of cytoskeleton proteins on the gene and protein levels in senescent and young fibroblasts. Their results show that senescent skin fibroblasts have an upregulated expression of the intermediate filament (IF) protein vimentin in contrast to actin and tubulin, which are downregulated. IFs play an important role in providing mechanical stability of cells. However, the mechanical properties of IFs depending on cellular senescence or age of the donor has not been studied so far. Hence, we employed passive microrheology on primary human dermal fibroblasts from female donors with age of 28 years (young) and 86 years (old) as model of in vivo aging and human normal dermal fibroblast from 11-year old male with CPD 17-35 (young) and CPD 58-59 (senescence) as a model of in vitro replicative senescence. In contrast to the expectations, our primary results show no significant differences in the viscoelastic properties of fibroblasts depending on age of the donor or cellular replicative senescence.

Keywords: aging, cytoskeleton, fibroblast, mechanical properties

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911 Phytochemical Constituents and Bioactive Properties of Glinus oppositifolius (L.) Aug. DC. against Bacterial Pathogens

Authors: Juliana Janet R. Martin-Puzon, Demetrio L. Valle, Windell L. Rivera

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This study aimed to determine the presence of bioactive phytochemical constituents and evaluate the in vitro antibacterial activities of Glinus oppositifolius or carpet weed, a plant valued for its use in traditional medicine and as a vegetable. The leaves, stems, and roots were extracted using chloroform, ethanol, and methanol. Phytochemical screening revealed that the entire G. oppositifolius plant, i.e. roots, stems, and leaves, is a rich source of alkaloids, flavonoids, glycosides, saponins, sterols, tannins, and triterpenes. The antibacterial activity of the leaf and stem extracts were evaluated through disc diffusion, minimum inhibitory concentration, and bactericidal concentration assays against methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant Enterococcus (VRE), extended spectrum β-lactamase-producing (ESβL+), carbapenem-resistant Enterobacteriaceae (CRE), and metallo-β-lactamase-producing (MβL+) Pseudomonas aeruginosa and Acinetobacter baumannii. The leaf extracts revealed antibacterial activities, inhibiting the growth of non-resistant and multidrug-resistant (MDR) strains of the Gram-negative bacteria E. coli, P. aeruginosa, and A. baumanii. In conclusion, the various biological activities of G. oppositifolius, including its antibacterial activity, are due to the presence of diverse bioactive secondary metabolites. The presence of phytochemical compounds in G. oppositifolius is scientific evidence on its use for treatment of many ailments. Thus, the results demonstrate the great potential of the plant as a new, alternative source of antimicrobials and other components with therapeutic value.

Keywords: antibacterial, Glinus oppositifolius, multidrug-resistant, secondary metabolites

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910 Biodegradable and Bioactive Scaffold for Bone Tissue Engineering

Authors: A. M. Malagon Escandon, J. A. Arenas Alatorre, C. P. Chaires Rosas, N. A. Vazquez Torres, B. Hernandez Tellez, G. Pinon Zarate, M. Herrera Enriquez, A. E. Castell Rodriguez

Abstract:

The current approach to the treatment of bone defects involves the use of scaffolds that provide a biological and mechanically stable niche to favor tissue repair. Despite the significant progress in the field of bone tissue engineering, several main problems associated are attributed to giving a low biodegradation degree, does not promote osseointegration and regeneration, if the bone is not healing as well as expected or fails to heal, will not be given a proper ossification or new bone formation. The actual approaches of bone tissue regeneration are directed to the use of decellularized native extracellular matrices, which are able of retain their own architecture, mechanic properties, biodegradability and promote new bone formation because they are capable of conserving proteins and other factors that are founded in physiological concentrations. Therefore, we propose an extracellular matrix-based bioscaffolds derived from bovine cancellous bone, which is processed by decellularization, demineralization, and hydrolysis of the collagen protein, these protocols have been successfully carried out in other organs and tissues; the effectiveness of its biosafety has also been previously evaluated in vivo and Food and Drug Administration (FDA) approved. In the specific case of bone, a more complex treatment is needed in comparison with other organs and tissues because is necessary demineralization and collagen denaturalization. The present work was made in order to obtain a temporal scaffold that succeed in degradation in an inversely proportional way to the synthesis of extracellular matrix and the maturation of the bone by the cells of the host.

Keywords: bioactive, biodegradable, bone, extracellular matrix-based bioscaffolds, stem cells, tissue engineering

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909 Evaluation of Synthesis and Structure Elucidation of Some Benzimidazoles as Antimicrobial Agents

Authors: Ozlem Temiz Arpaci, Meryem Tasci, Hakan Goker

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Benzimidazole, a structural isostere of indol and purine nuclei that can interact with biopolymers, can be identified as master key. So that benzimidazole compounds are important fragments in medicinal chemistry because of their wide range of biological activities including antimicrobial activity. We planned to synthesize some benzimidazole compounds for developing new antimicrobial drug candidates. In this study, we put some heterocyclic rings on second position and an amidine group on the fifth position of benzimidazole ring and synthesized them using a multiple step procedure. For the synthesis of the compounds, as the first step, 4-chloro-3-nitrobenzonitrile was reacted with cyclohexylamine in dimethyl formamide. Imidate esters (compound 2) were then prepared with absolute ethanol saturated with dry HCl gas. These imidate esters which were not too stable were converted to compound 3 by passing ammonia gas through ethanol. At the Pd / C catalyst, the nitro group is reduced to the amine group (compound 4). Finally, various aldehyde derivatives were reacted with sodium metabisulfite addition products to give compound 5-20. Melting points were determined on a Buchi B-540 melting point apparatus in open capillary tubes and are uncorrected. Elemental analyses were done a Leco CHNS 932 elemental analyzer. 1H-NMR and 13C-NMR spectra were recorded on a Varian Mercury 400 MHz spectrometer using DMSO-d6. Mass spectra were acquired on a Waters Micromass ZQ using the ESI(+) method. The structures of them were supported by spectral data. The 1H-NMR, 13C NMR and mass spectra and elemental analysis results agree with those of the proposed structures. Antimicrobial activity studies of the synthesized compounds are under the investigation.

Keywords: benzimidazoles, synthesis, structure elucidation, antimicrobial

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908 Electrochemical Detection of the Chemotherapy Agent Methotrexate in vitro from Physiological Fluids Using Functionalized Carbon Nanotube past Electrodes

Authors: Shekher Kummari, V. Sunil Kumar, K. Vengatajalabathy Gobi

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A simple, cost-effective, reusable and reagent-free electrochemical biosensor is developed with functionalized multiwall carbon nanotube paste electrode (f-CNTPE) for the sensitive and selective determination of the important chemotherapeutic drug methotrexate (MTX), which is widely used for the treatment of various cancer and autoimmune diseases. The electrochemical response of the fabricated electrode towards the detection of MTX is examined by cyclic voltammetry (CV), differential pulse voltammetry (DPV) and square wave voltammetry (SWV). CV studies have shown that f-CNTPE electrode system exhibited an excellent electrocatalytic activity towards the oxidation of MTX in phosphate buffer (0.2 M) compared with a conventional carbon paste electrode (CPE). The oxidation peak current is enhanced by nearly two times in magnitude. Applying the DPV method under optimized conditions, a linear calibration plot is achieved over a wide range of concentration from 4.0×10⁻⁷ M to 5.5×10⁻⁶ M with the detection limit 1.6×10⁻⁷ M. further, by applying the SWV method a parabolic calibration plot was achieved starting from a very low concentration of 1.0×10⁻⁸ M, and the sensor could detect as low as 2.9×10⁻⁹ M MTX in 10 s and 10 nM were detected in steady state current-time analysis. The f-CNTPE shows very good selectivity towards the specific recognition of MTX in the presence of important biological interference. The electrochemical biosensor detects MTX in-vitro directly from pharmaceutical sample, undiluted urine and human blood serum samples at a concentration range 5.0×10⁻⁷ M with good recovery limits.

Keywords: amperometry, electrochemical detection, human blood serum, methotrexate, MWCNT, SWV

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907 Design and Synthesis of Some Oxadiazole Bearing Benzimidazole Derivatives as Potential Epidermal Growth Factor Receptor Inhibitors

Authors: Ismail Celik, Gulgun Ayhan Kilcigil, Berna Guven, Zumra Kara, Arzu Onay-Besikci

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Epidermal Growth Factor Receptor is the cell-surface receptor of the ErbB (erythroblastic leukemia viral oncogene homologue receptors) family of tyrosine kinases. It plays a vital role in regulating the proliferation and differentiation of cells. However, a variety of mechanisms, such as EGFR expression, mutation, and ligand-dependent receptor dimerization, are associated with the development of various activated EGFR tumors. EGFR is highly expressed in most solid tumors, including breast, head and neck cancer, non-small cell lung cancer (NSCLC), renal, ovarian, and colon cancers. Thus, specific EGFR inhibition plays one of the key roles in cancer treatment. The compounds used in the treatment as tyrosine kinase inhibitors are known to contain the benzimidazole isosterium indole, pazopanib, and axitinibin indazole rings. In addition, benzimidazoles have been shown to exhibit protein kinase inhibitory activity in addition to their different biological activities.Based on these data, it was planned and synthesized of some oxadiazole bearing benzimidazole derivatives [N-cyclohexyl-5-((2-phenyl/substitutedphenyl-1H-benzo[d]imidazole-1-yl) methyl)-1,3,4-oxadiazole-2-amine]. EGFR kinase inhibitory efficiency of the synthesized compounds was determined by comparing them with a known kinase inhibitor erlotinib in vitro, and two of the compounds bearing phenyl (19a) and 3,4-dibenzyloxyphenyl (21a) ring exhibited significant activities.

Keywords: benzimidazole, EGFR kinase inhibitory, oxadiazole, synthesis

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