Search results for: bioactive agents

Authors: O. J. Jesumoroti, Faridoon, R. Klein, K. A. Iobb, D. Mnkadhla, H. C. Hoppe, P. T. Kaye

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The 1, 3-aryl diketo acids (DKA) based agents represent an important class of HIV integrase (IN) strand transfer inhibitors. In other to study the chelating role of the divalent metal ion in the inhibition of IN strand transfer, we designed and synthesized a series of 2-hydroxy-3-oxo-3-phenyl propionate derivatives with the notion that such compounds could interact with the divalent ion in the active site of IN. The synthetic sequence to the desired compounds involves the concept of Doebner knoevenagel condensation, Fischer esterification and ketohydroxylation using neuclophilic re-oxidant; compounds were characterized by their IR, IHNMR, 13CNMR, HRMS spectroscopic data and melting point determination. Also, molecular docking was employed in this study and it was revealed that there is interaction with the active site of the enzyme. However, there is disparity in the corresponding anti-HIV activity determined by the experimental bioassay. These compounds lack potency at low micromolar concentration when compared to the results of the docking studies. Nevertheless, the results of the study suggest modification of the aryl ring with one or two hydroxyl groups to improve the inhibitory activity.

Keywords: anti-HIV-1 integrase, ketohydroxylation, molecular docking, propionate derivatives

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Authors: David Guillermo Piedrahita Marquez, Hector Suarez Mahecha, Jairo Humberto Lopez

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The propolis are substances obtained from the beehive have an action against pathogens, prooxidant substances and free radicals because of its polyphenols content, this has motivated the use of these compounds in the food and pharmaceutical industries. However, due to their organoleptic properties and their ability to react with other compounds, their application has been limited; therefore, the objective of this research was to propose a mechanism to protect propolis and mitigate side effects granted by its components. To achieve the stated purpose ethanolic extracts of propolis (EEP) from three samples from Santander were obtained and their antioxidant and antimicrobial activity were evaluated in order to choose the extract with the biggest potential. Subsequently mixtures of the extract with maltodextrin were prepared by spray drying varying concentration and temperature, finally the yield, the physicochemical, and antioxidant properties of the products were measured. It was concluded that Socorro propolis was the best for the production of microencapsulated due to their activity against pathogenic strains, for its large percentage of DPPH radical inactivation and for its high phenolic content. In spray drying, the concentration of bioactive had a greater impact than temperature and the conditions set allowed a good performance and the production of particles with high antioxidant potential and little chance of proliferation of microorganisms. Also, it was concluded that the best conditions that allowed us to obtain the best particles were obtained after drying a mixture 1:2 ( EEP: Maltodextrin), besides the concentration is the most important variable in the spray drying process, at the end we obtained particles of different sizes and shape and the uniformity of the surface depend on the temperature. After watching the previously mentioned microparticles by scanning electron microscopy (SEM) it was concluded that most of the particles produced during the spray dry process had a spherical shape and presented agglomerations due to the moisture content of the ethanolic extracts of propolis (EEP), the morphology of the microparticles contributed to the stability of the final product and reduce the loss of total phenolic content.

Keywords: spray drying, propolis, maltodextrin, encapsulation, scanning electron microscopy

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Authors: Frank Boris Feutmba Keutchou, Saurelle Fabienne Bieghan Same, Verelle Elsa Fogang Pokam, Charles Ursula Metapi Meikeu, Angel Marilyne Messop Nzomo, Ousman Tamgue

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Infectious diseases are one of the most important causes of morbidity and mortality worldwide. These diseases are caused by micro-pathogenic organisms, such as bacteria, viruses, parasites, and fungi. Heritable changes in gene expression that do not involve changes to the underlying DNA sequence are referred to as epigenetics. Emerging evidence suggests that epigenetic mechanisms are important in the emergence and progression of infectious diseases. Pathogens can manipulate host epigenetic machinery to promote their own replication and evade immune responses. The Human Genome Project has provided new opportunities for developing better tools for the diagnosis and identification of target genes. Several epigenetic modifications, such as DNA methylation, histone modifications, and non-coding RNA expression, have been shown to influence infectious disease outcomes. Understanding the epigenetic mechanisms underlying infectious diseases may result in the progression of new therapeutic approaches focusing on host-pathogen interactions. The goal of this study is to show how different infectious agents interact with host cells after infection.

Keywords: epigenetic, infectious disease, micro-pathogenic organism, phenotype

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Authors: Fevy Kae Mateo, Kimberly Javier, Alyzza Marie Palles

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Leadership is a process of relationship involving interaction with other people. Leaders emphasise authority, which executes and implements regulations, maintains the rules and leads to a better future. The First Time voters are very significant because there are the stakeholders of the type of leader to be deployed. They also have the capacity of engaging the government and can be the agents of change. The objective of the study is to identify the strengths and weaknesses of leader. Moreover, the study identifies the qualities of a leader. Finally, the study determines first-time voter’s representation of a leader. Focus Group Discussion was carried out into two groups of first time voter’s ages 18 to 21 years old. Verbatim transcripts of the discussion were analyzed using Thematic Analysis. Overall results showed super ordinate themes for weaknesses of leader: Lace of transparency in the government, poor communication strategy, and valuing experience over potential and other contributory factor; for strength of a leader: analytical skill, emotional intelligence in political work, analytical ability and economic status on political participation; finally, in the representation of a leader: positive representation of a leader and negative representation of a leader.

Keywords: first time voters, focus group discussion, leadership, qualitative research design

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Authors: Mallikarjun B. Channappagoudar, Pallapa Venkataram

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The dynamic nature of Mobile adhoc network (MANET) due to mobility and disconnection of mobile nodes, leads to various problems in predicting the movement of nodes and their location information updation, for efficient interaction among the application specific nodes. Location management is one of the main challenges to be considered for an efficient service provision to the applications of a MANET. In this paper, we propose a location management protocol, for locating the nodes of a MANET and to maintain uninterrupted high-quality service for distributed applications by intelligently anticipating the change of location of its nodes. The protocol predicts the node movement and application resource scarcity, does the replacement with the chosen nodes nearby which have less mobility and rich in resources, with the help of both static and mobile agents, and maintains the application continuity by providing required network resources. The protocol has been simulated using Java Agent Development Environment (JADE) Framework for agent generation, migration and communication. It consumes much less time (response time), gives better location accuracy, utilize less network resources, and reduce location management overhead.

Keywords: mobile agent, location management, distributed applications, mobile adhoc network

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Authors: J. Skibinski, P. Caban, T. Wejrzanowski, K. J. Kurzydlowski

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In the present study numerical simulations of epitaxial growth of gallium nitride in Metal Organic Vapor Phase Epitaxy reactor AIX-200/4RF-S are addressed. The aim of this study was to design the optimal fluid flow and thermal conditions for obtaining the most homogeneous product. Since there are many agents influencing reactions on the crystal growth area such as temperature, pressure, gas flow or reactor geometry, it is difficult to design optimal process. Variations of process pressure and hydrogen mass flow rates have been considered. According to the fact that it’s impossible to determine experimentally the exact distribution of heat and mass transfer inside the reactor during crystal growth, detailed 3D modeling has been used to get an insight of the process conditions. Numerical simulations allow to understand the epitaxial process by calculation of heat and mass transfer distribution during growth of gallium nitride. Including chemical reactions in the numerical model allows to calculate the growth rate of the substrate. The present approach has been applied to enhance the performance of AIX-200/4RF-S reactor.

Keywords: computational fluid dynamics, finite volume method, epitaxial growth, gallium nitride

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Authors: Kaouka Alaeddine, K. Benarous

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This study aims to obtain a surface of pure titanium and titanium alloy Ti-64Al with high performance by the diffusion process. Two agents metal alloy have been used in this treatment, niobium (Nb) and molybdenum (Mo), spread on elemental titanium and Ti-64Al alloy. Nb and Mo are used as powder form to increase the contact surface and to improve the distribution. Both Mo and Nb are distributed on samples of Ti and Ti-64Al at 1100 °C and 1200 °C for 3 h. They were performed to effect different experiments objectives. This work was achieved to improve some properties and microstructure of Ti and Ti-64Al surface, using optical microscopy and SEM and study some mechanical properties. The effects of temperature and the powder contents on the microstructure of Ti and Ti-64Al alloy, different phases and hardness value of Ti and Ti-64Al alloy were determined. Experimental results indicate that increasing the powder contents and/or the temperature, the α + β phases change to the equiaxed β lamellar structure. In particular, experiments in 1200 °C were created by diffusion α + β phases both equiaxed β phase laminar and α + β phase, thus meeting the objectives were established in the work. In addition, simulation results are used for comparison with the experimental results by DICTRA software.

Keywords: diffusion, powder metallurgy, titanium alloy, molybdenum, niobium

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Authors: M. Kumpugdee-Vollrath, J.-P. Krause, S. Bürk

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Most of the drugs used for pharmaceutical purposes are poorly water-soluble drugs. About 40% of all newly discovered drugs are lipophilic and the numbers of lipophilic drugs seem to increase more and more. Drug delivery systems such as nanoparticles, micelles or liposomes are applied to improve their solubility and thus their bioavailability. Besides various techniques of solubilization, oil-in-water emulsions are often used to incorporate lipophilic drugs into the oil phase. To stabilize emulsions surface active substances (surfactants) are generally used. An alternative method to avoid the application of surfactants was of great interest. One possibility is to develop O/W-emulsion without any addition of surface active agents or the so called “surfactant-free emulsion or SFE”. The aim of this study was to develop and characterize SFE as a drug carrier by varying the production conditions. Lidocaine base was used as a model drug. The injection method was developed. Effects of ultrasound as well as of temperature on the properties of the emulsion were studied. Particle sizes and release were determined. The long-term stability up to 30 days was performed. The results showed that the surfactant-free O/W emulsions with pharmaceutical oil as drug carrier can be produced.

Keywords: emulsion, lidocaine, Miglyol, size, surfactant, light scattering, release, injection, ultrasound, stability

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Authors: Vera Lukasova, Eva Filova, Jana Dankova, Vera Sovkova, Matej Daniel, Michala Rampichova

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Proper bone implants should promote fast adhesion of cells, stimulate cell differentiation and support the formation of bone tissue. Nowadays titanium is used as a biocompatible material capable of bone tissue integration. This study was focused on comparison of bioactive properties of two titanium alloys - beta titanium alloy Ti36Nb6Ta and standard medical titanium alloy Ti6A14V. The advantage of beta titanium alloy Ti36Nb6Ta is mainly that this material does not contain adverse elements like vanadium or aluminium. Titanium alloys were sterilized in ethanol, placed into 48 well plates and seeded with porcine mesenchymal stem cells. Cells were cultivated for 14 days in standard growth cultivation media with osteogenic supplements. Cell metabolic activity was quantified using MTS assay (Promega). Cell adhesion on day 1 and cell proliferation on further days were verified immunohistochemically using beta-actin monoclonal antibody and secondary antibody conjugated with AlexaFluor®488. Differentiation of cells was evaluated using alkaline phosphatase assay. Additionally, gene expression of collagen I was measured by qRT-PCR. Porcine mesenchymal stem cells adhered and spread well on beta titanium alloy Ti36Nb6Ta on day 1. During the 14 days’ time period the cells were spread confluently on the surface of the beta titanium alloy Ti36Nb6Ta. The metabolic activity of cells increased during the whole cultivation period. In comparison to standard medical titanium alloy Ti6A14V, we did not observe any differences. Moreover, the expression of collagen I gene revealed no statistical differences between both titanium alloys. Therefore, a beta titanium alloy Ti36Nb6Ta promotes cell adhesion, metabolic activity, proliferation and collagen I expression equally to standard medical titanium alloy Ti6A14V. Thus, beta titanium is a suitable material that provides sufficient biocompatible properties. This project was supported by the Czech Science Foundation: grant No. 16-14758S.

Keywords: beta titanium alloy, biocompatibility, differentiation, mesenchymal stem cells

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Authors: Nur Aimi Syairah Mohd Abdul Alim, Azilah Ajit, A. Z. Sulaiman

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The present study aimed to investigate the effects of ultrasound-assisted extraction (UAE) on the extraction of Vitexin and Iso-Vitexin from Ficus deltoidea plants. In recent years, ultrasound technology has been found to be a potential herbal extraction technique. The passage of ultrasound energy in a liquid medium generates mechanical agitation and other physical effects due to acoustic cavitation. The main goal is to optimised ultrasonic-assisted extraction condition providing the highest extraction yield with the most desirable antioxidant activity and stability. Thus, a series of experiments has been developed to investigate the effect of ultrasound energy on the vegetal material and the implemented parameters by using HPLC-photodiode array detection. The influences of several experimental parameters on the ultrasonic extraction of Ficus deltoidea leaves were investigated: extraction time (1-8 h), solvent-to-water ratio (1:10 to 1:50), temperature (50–100 °C), duty cycle (10–continuous sonication) and intensity. The extracts at the optimized condition were compared with those obtained by conventional boiling extraction, in terms of bioactive constituents yield and chemical composition. The compounds of interest identified in the extracts were Vitexin and Isovitexin, which possess anti-diabetic, anti-oxidant and anti-cancer properties. Results showed that the main variables affecting the extraction process were temperature and time. Though in less extent, solvent-to-water ratio, duty cycle and intensity are also demonstrated to be important parameters. The experimental values under optimal conditions were in good consistent with the predicted values, which suggested that ultrasonic-assisted extraction (UAE) is more efficient process as compared to conventional boiling extraction. It recommended that ultrasound extraction of Ficus deltoidea plants are feasible to replace the traditional time-consuming and low efficiency preparation procedure in the future modernized and commercialized manufacture of this highly valuable herbal medicine.

Keywords: Ficus, ultrasounds, vitexin, isovitexin

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Authors: Varsha Gupta, Priya Datta, Gursimran Mohi, Jagdish Chander

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Fluoroquinolones form the mainstay of therapy for the treatment of infections due to Salmonella enterica subsp. enterica. There is a complex interplay between several resistance mechanisms for quinolones and various fluoroquinolones discs, giving varying results, making detection and interpretation of fluoroquinolone resistance difficult. For detection of fluoroquinolone resistance in Salmonella ssp., we compared the use of pefloxacin and nalidixic acid discs as surrogate marker. Using MIC for ciprofloxacin as the gold standard, 43.5% of strains showed MIC as ≥1 μg/ml and were thus resistant to fluoroquinoloes. Based on the performance of nalidixic acid and pefloxacin discs as surrogate marker for ciprofloxacin resistance, both the discs could correctly detect all the resistant phenotypes; however, use of nalidixic acid disc showed false resistance in the majority of the sensitive phenotypes. We have also tested newer antimicrobial agents like cefixime, imipenem, tigecycline and azithromycin against Salmonella spp. Moreover, there was a comeback of susceptibility to older antimicrobials like ampicillin, chloramphenicol, and cotrimoxazole. We can also use cefixime, imipenem, tigecycline and azithromycin in the treatment of multidrug resistant S. typhi due to their high susceptibility.

Keywords: salmonella, pefloxacin, surrogate marker, chloramphenicol

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Authors: Maryam Ehsanpou, Majid Afkhami, Flora Mohammadizadeh, Amirhoushang Bahri, Rastin Afkhami

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Within the frame of a biodiversity and bioactivity study of marine macro organisms from the Persian Gulf, three hard coral species extracts were investigated for cytotoxic, antibacterial and antifungal activities against five human pathogenic microorganisms. All concentrations of extracts from three hard corals showed no antifungal activity towards the tested strains. In antibacterial assays, the hard coral extracts showed significant activity solely against Staphylococcus aureus with MICs ranging from 3 to 9 μg/ml. The highest antibacterial activity was found in the aqueous methanol extract of Porites compressa with an inhibition zone of 22 mm against Staphylococcus aureus at 18 μg/ml extract concentration. Methanol extracts from Porites harrisoi and Porites compressa exhibited only weak cytotoxic activities. It is important for future research to concentrate on finding the mechanisms employed by corals to defend themselves against invasion, the mechanism of infections and the type of chemical compounds in coral extracts that inhibit antibacterial growth or proliferation in underexplored areas such as the Persian Gulf.

Keywords: antibacterial, antifungal, cytotoxic, hard corals, Persian Gulf

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Authors: M.Ayazi, N. Golshan Ebrahimi

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The development of antibacterial surface has devoted extensive researches and important field due to the growing antimicrobial resistance strains. The superhydrophobic surface has raised attention because of reducing bacteria adhesion in the absence of antibiotic agents. Evaluating the current development antibacterial surface has to be investigating to consider the potential of applying superhydrophobic surface to reduce bacterial adhesion or role of patterned surfaces on it. In this study, we present different samples with bio-inspired hierarchical and microstructures to consider their ability in reducing bacterial adhesion. The structures have inspired from rice-like pattern and lotus-leaf that developed on the polydimethylsiloxane (PDMS) and polypropylene (PP). The results of the attachment behaviors have considered on two bacteria strains of gram-negative Escherichia coli (E. coli) bacteria and gram-positive Staphylococcus aureus (S. aureus). The reduction of bacteria adhesion on these roughness surfaces demonstrated the effectiveness of rinsing ability on removing bacterial cells on structured plastic surfaces. Results have also offered the important role of bacterial species, material chemistry and hierarchical structure to prevent bacterial adhesion.

Keywords: hierarchical structure, self-cleaning, lotus-effect, bactericidal

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Authors: Asim Abbasi, Muhammad Sufyan, Iqra, Hafiza Javaria Ashraf

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The share of vector-borne diseases (VBDs) in the global burden of infectious diseases is almost 17%. The advent of new drugs and latest research in medical science helped mankind to compete with these lethal diseases but still diseases transmitted by different mosquito species, including filariasis, malaria, viral encephalitis and dengue are serious threats for people living in disease endemic areas. Injudicious and repeated use of pesticides posed selection pressure on mosquitoes leading to development of resistance. Hence biological control agents are under serious consideration of scientific community to be used in vector control programmes. Fish have a history of predating immature stages of different aquatic insects including mosquitoes. The noteworthy examples in Africa and Asia includes, Aphanius discolour and a fish in the Panchax group. Moreover, common mosquito fish, Gambusia affinis predates mostly on temporary water mosquitoes like anopheline as compared to permanent water breeders like culicines. Mosquitoes belonging to genus Toxorhynchites have a worldwide distribution and are mostly associated with the predation of other mosquito larvae habituating with them in natural and artificial water containers. These species are harmless to humans as their adults do not suck human blood but feeds on floral nectar. However, their activity is mostly temperature dependent as Toxorhynchites brevipalpis consume 359 Aedes aegypti larvae at 30-32 ºC in contrast to 154 larvae at 20-26 ºC. Although many bacterial species were isolated from mosquito cadavers but those belonging to genus Bacillus are found highly pathogenic against them. The successful species of this genus include Bacillus thuringiensis and Bacillus sphaericus. The prime targets of B. thuringiensis are mostly the immatures of genus Aedes, Culex, Anopheles and Psorophora while B. sphaericus is specifically toxic against species of Culex, Psorophora and Culiseta. The entomopathogenic nematodes belonging to family, mermithidae are also pathogenic to different mosquito species. Eighty different species of mosquitoes including Anopheles, Aedes and Culex proved to be highly vulnerable to the attack of two mermithid species, Romanomermis culicivorax and R. iyengari. Cytoplasmic polyhedrosis virus was the first described pathogenic virus, isolated from the cadavers of mosquito specie, Culex tarsalis. Other viruses which are pathogenic to culicine includes, iridoviruses, cytopolyhedrosis viruses, entomopoxviruses and parvoviruses. Protozoa species belonging to division microsporidia are the common pathogenic protozoans in mosquito populations which kill their host by the chronic effects of parasitism. Moreover, due to their wide prevalence in anopheline mosquitoes and transversal and horizontal transmission from infected to healthy host, microsporidia of the genera Nosema and Amblyospora have received much attention in various mosquito control programmes. Fungal based mycopesticides are used in biological control of insect pests with 47 species reported virulent against different stages of mosquitoes. These include both aquatic fungi i.e. species of Coelomomyces, Lagenidium giganteum and Culicinomyces clavosporus, and the terrestrial fungi Metarhizium anisopliae and Beauveria bassiana. Hence, it was concluded that the integrated use of all these biological control agents can be a healthy contribution in mosquito control programmes and become a dire need of the time to avoid repeated use of pesticides.

Keywords: entomopathogenic nematodes, protozoa, Toxorhynchites, vector-borne

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

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The complexes of transition metals with various organic ligands have been extensively studied as models of some important pharmaceutical molecules. It was found that biological properties of different substituted organic molecules are improved when they are complexed by different metals. Therefore, it is of great importance for the development of coordination chemistry to explore the assembly of functional organic ligands with metal ion and to investigate the relationship between the structure and property. In the present work, we have bioassayed the antibacterial potency of benzimidazoles and their metal salts (Cu or Zn) against yeast Sarcina lutea. In order to validate our in vitro study, we performed in silico studies using molecular docking software. The investigated compounds and their metal complexes (Cu, Zn) showed good to moderate inhibitory activity against Sarcina lutea. In silico docking studies of the synthesized compounds suggested that complexed benzimidazoles have a greater binding affinity and improved antibacterial activity in comparison with non-complexed ligands. These results are part of the CMST COST Action No. 1105 "Functional metal complexes that bind to biomolecules".

Keywords: organometallic complexes, benzimidazoles, chemometric design, Sarcina lutea

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Authors: Issa M. Hweidi, Saba W. Al-Ibraheem

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This study aimed to assess the increased hospital length of stay and healthcare costs associated with SSIs among ventriculoperitoneal shunting surgery patients in Jordan. This study adopted a retrospective and nested 1:1 matched case-control design. A non-probability convenient sample of 48 VP shunt patients was recruited for the purpose of the study. The targeted groups of the study basically used to cross-match the variables investigated to minimize the risk of confounding. Information was extracted from the text of patients' electronic health records. As compared to the non-SSI group, the SSI group had an extra mean healthcare cost of $13,696.53 (p=0.001) and longer hospital length of stay (22.64 mean additional days). Furthermore, Acinetobacter baumannii and Klebsiella pneumonia were identified as being the most predominant causative agents of SSIs. The results of this study may provide baseline data for national and regional benchmarking to evaluate the quality of care provided to likewise patients. Adherence to infection control strategies and protocols considering new surveillance methods of SSIs is encouraged.

Keywords: ventriculoperitoneal shunt, health care cost, length of stay, neurosurgery, surgical site infections

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Authors: Mariia V. Efremova, Iana O. Tcareva, Anastasia D. Blokhina, Ivan S. Grebennikov, Anastasia S. Garanina, Maxim A. Abakumov, Yury I. Golovin, Alexander G. Savchenko, Alexander G. Majouga, Natalya L. Klyachko

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During last decades magnetite nanoparticles (NPs) attract a deep interest of scientists due to their potential application in therapy and diagnostics. However, magnetite nanoparticles are toxic and non-stable in physiological conditions. To solve these problems, we decided to create two types of hybrid systems based on magnetite and gold which is inert and biocompatible: gold as a shell material (first type) and gold as separate NPs interfacially bond to magnetite NPs (second type). The synthesis of the first type hybrid nanoparticles was carried out as follows: Magnetite nanoparticles with an average diameter of 9±2 nm were obtained by co-precipitation of iron (II, III) chlorides then they were covered with gold shell by iterative reduction of hydrogen tetrachloroaurate with hydroxylamine hydrochloride. According to the TEM, ICP MS and EDX data, final nanoparticles had an average diameter of 31±4 nm and contained iron even after hydrochloric acid treatment. However, iron signals (K-line, 7,1 keV) were not localized so we can’t speak about one single magnetic core. Described nanoparticles covered with mercapto-PEG acid were non-toxic for human prostate cancer PC-3/ LNCaP cell lines (more than 90% survived cells as compared to control) and had high R2-relaxivity rates (>190 mМ-1s-1) that exceed the transverse relaxation rate of commercial MRI-contrasting agents. These nanoparticles were also used for chymotrypsin enzyme immobilization. The effect of alternating magnetic field on catalytic properties of chymotrypsin immobilized on magnetite nanoparticles, notably the slowdown of catalyzed reaction at the level of 35-40 % was found. The synthesis of the second type hybrid nanoparticles also involved two steps. Firstly, spherical gold nanoparticles with an average diameter of 9±2 nm were synthesized by the reduction of hydrogen tetrachloroaurate with oleylamine; secondly, they were used as seeds during magnetite synthesis by thermal decomposition of iron pentacarbonyl in octadecene. As a result, so-called dumbbell-like structures were obtained where magnetite (cubes with 25±6 nm diagonal) and gold nanoparticles were connected together pairwise. By HRTEM method (first time for this type of structure) an epitaxial growth of magnetite nanoparticles on gold surface with co-orientation of (111) planes was discovered. These nanoparticles were transferred into water by means of block-copolymer Pluronic F127 then loaded with anti-cancer drug doxorubicin and also PSMA-vector specific for LNCaP cell line. Obtained nanoparticles were found to have moderate toxicity for human prostate cancer cells and got into the intracellular space after 45 minutes of incubation (according to fluorescence microscopy data). These materials are also perspective from MRI point of view (R2-relaxivity rates >70 mМ-1s-1). Thereby, in this work magnetite-gold hybrid nanoparticles, which have a strong potential for biomedical application, particularly in targeted drug delivery and magnetic resonance imaging, were synthesized and characterized. That paves the way to the development of special medicine types – theranostics. The authors knowledge financial support from Ministry of Education and Science of the Russian Federation (14.607.21.0132, RFMEFI60715X0132). This work was also supported by Grant of Ministry of Education and Science of the Russian Federation К1-2014-022, Grant of Russian Scientific Foundation 14-13-00731 and MSU development program 5.13.

Keywords: drug delivery, magnetite-gold, MRI contrast agents, nanoparticles, toxicity

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Authors: Viviana Manzulli, Luigina Serrecchia, Adelia Donatiello, Valeria Rondinone, Sabine Zange, Alina Tscherne, Antonio Parisi, Antonio Fasanella

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Anthrax is a zoonotic disease that affects a wide range of animal species (primarily ruminant herbivores), and can be transmitted to humans through consumption or handling of contaminated animal products. The etiological agent B.anthracis is able to survive in unfavorable environmental conditions by forming endospore which remain viable in the soil for many decades. Furthermore, B.anthracis is considered as one of the most feared agents to be potentially misused as a biological weapon and the importance of the disease and its treatment in humans has been underscored before the bioterrorism events in the United States in 2001. Due to the often fatal outcome of human cases, antimicrobial susceptibility testing plays especially in the management of anthrax infections an important role. In Italy, animal anthrax is endemic (predominantly found in the southern regions and on islands) and is characterized by sporadic outbreaks occurring mainly during summer. Between 2012 and 2017 single human cases of cutaneous anthrax occurred. In this study, 90 diverse strains of B.anthracis, isolated in Italy from 2001 to 2017, were screened to their susceptibility to sixteen clinically relevant antimicrobial agents by using the broth microdilution method. B.anthracis strains selected for this study belong to the strain collection stored at the Anthrax Reference Institute of Italy located inside the Istituto Zooprofilattico Sperimentale of Puglia and Basilicata. The strains were isolated at different time points and places from various matrices (human, animal and environmental). All strains are a representative of over fifty distinct MLVA 31 genotypes. The following antibiotics were used for testing: gentamicin, ceftriaxone, streptomycin, penicillin G, clindamycin, chloramphenicol, vancomycin, linezolid, cefotaxime, tetracycline, erythromycin, rifampin, amoxicillin, ciprofloxacin, doxycycline and trimethoprim. A standard concentration of each antibiotic was prepared in a specific diluent, which were then twofold serial diluted. Therefore, each wells contained: bacterial suspension of 1–5x104 CFU/mL in Mueller-Hinton Broth (MHB), the antibiotic to be tested at known concentration and resazurin, an indicator of cell growth. After incubation overnight at 37°C, the wells were screened for color changes caused by the resazurin: a change from purple to pink/colorless indicated cell growth. The lowest concentration of antibiotic that prevented growth represented the minimal inhibitory concentration (MIC). This study suggests that B.anthracis remains susceptible in vitro to many antibiotics, in addition to doxycycline (MICs ≤ 0,03 µg/ml), ciprofloxacin (MICs ≤ 0,03 µg/ml) and penicillin G (MICs ≤ 0,06 µg/ml), recommend by CDC for the treatment of human cases and for prophylactic use after exposure to the spores. In fact, the good activity of gentamicin (MICs ≤ 0,25 µg/ml), streptomycin (MICs ≤ 1 µg/ml), clindamycin (MICs ≤ 0,125 µg/ml), chloramphenicol(MICs ≤ 4 µg/ml), vancomycin (MICs ≤ 2 µg/ml), linezolid (MICs ≤ 2 µg/ml), tetracycline (MICs ≤ 0,125 µg/ml), erythromycin (MICs ≤ 0,25 µg/ml), rifampin (MICs ≤ 0,25 µg/ml), amoxicillin (MICs ≤ 0,06 µg/ml), towards all tested B.anthracis strains demonstrates an appropriate alternative choice for prophylaxis and/or treatment. All tested B.anthracis strains showed intermediate susceptibility to the cephalosporins (MICs ≥ 16 µg/ml) and resistance to trimethoprim (MICs ≥ 128 µg/ml).

Keywords: Bacillus anthracis, antibiotic susceptibility, treatment, minimum inhibitory concentration

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Authors: Fuad Abdullah Alatawi

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Microbial infections-based diseases are a significant public health issue around the world, mainly when antibiotic-resistant bacterium types evolve. In this research, we explored the anti-bacterial and anti-cancer potency of iron-oxide (Fe₂O₃) nanoparticles prepared from F. macrocarpa fruit extract. The chemical composition of F. macrocarpa fruit extract was used as a reducing and capping agent for nanoparticles’ synthesis was examined by GC-MS/MS analysis. Then, the prepared nanoparticles were confirmed by various biophysical techniques, including X-ray powder diffraction (XRD), Fourier-transform infrared spectroscopy (FTIR), UV-Vis Spectroscopy, and Transmission Electron Microscopy (TEM) and Energy Dispersive Spectroscopy (EDAX), and Dynamic Light Scattering (DLS). Also, the antioxidant capacity of fruit extract was determined through 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid (ABTS), Fluorescence Recovery After Photobleaching (FRAP), Superoxide Dismutase (SOD) assays. Furthermore, the cytotoxicity activities of Fe₂O₃ NPs were determined using the (3-(4, 5-dimethylthiazolyl-2)-2, 5-diphenyltetrazolium bromide) (MTT) test on MCF-7 cells. In the antibacterial assay, lethal doses of the Fe₂O₃NPs effectively inhibited the growth of gram-negative and gram-positive bacteria. The surface damage, ROS production, and protein leakage are the antibacterial mechanisms of Fe₂O₃NPs. Concerning antioxidant activity, the fruit extracts of F. macrocarpa had strong antioxidant properties, which were confirmed by DPPH, ABTS, FRAP, and SOD assays. In addition, the F. microcarpa-derived iron oxide nanomaterials greatly reduced the cell viability of (MCF-7). The GC-MS/MS analysis revealed the presence of 25 main bioactive compounds in the F. microcarpa extract. Overall, the finding of this research revealed that F. microcarpa-derived Fe₂O₃ nanoparticles could be employed as an alternative therapeutic agent to cure microbial infection and breast cancer in humans.

Keywords: ficus microcarpa, iron oxide, antibacterial activity, cytotoxicity

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Authors: T. Wanyama, B. Far

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Automatic irrigation systems usually conveniently protect landscape investment. While conventional irrigation systems are known to be inefficient, automated ones have the potential to optimize water usage. In fact, there is a new generation of irrigation systems that are smart in the sense that they monitor the weather, soil conditions, evaporation and plant water use, and automatically adjust the irrigation schedule. In this paper, we present an agent based smart irrigation system. The agents are built using a mix of commercial off the shelf software, including MATLAB, Microsoft Excel and KEPServer Ex5 OPC server, and custom written code. The Irrigation Scheduler Agent uses fuzzy logic to integrate the information that affect the irrigation schedule. In addition, the Multi-Agent system uses Open Platform Connectivity (OPC) technology to share data. OPC technology enables the Irrigation Scheduler Agent to communicate over the Internet, making the system scalable to a municipal or regional agent based water monitoring, management, and optimization system. Finally, this paper presents simulation and pilot installation test result that show the operational effectiveness of our system.

Keywords: community water usage, fuzzy logic, irrigation, multi-agent system

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Authors: Mir Afzal Tajik

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The 'Strengthening Teacher Education in Pakistan' (STEP) is an innovative programme jointly funded by the Government of Canada and the Aga Khan Foundation Canada and implemented by the Aga Khan University - Institute for Educational Development (AKU-IED) in partnership with the local governments, education departments and communities in the provinces of Balochistan, Sindh and Gilgit-Baltistan in Pakistan. One of the key components of the programme is the professional development of teachers, headteachers and teacher educators through a variety of teacher education programmes including a two-year Masters of Education (MEd) Programme offered by AKU-IED. A number of teachers, headteachers and teacher educators from these provinces have been developed through the MEd Programme. This paper discusses a qualitative research study conducted to explore the nature, relevance, rigor and richness of the experiences of the MEd graduates, and how these experiences have fostered their own professional development and their ability to bring about positive changes in their schools. The findings of the study provide useful insights into the graduates’ self-actualization, the transformation of their professional beliefs and practices, the difference they have made in their schools, and the challenges they face. The study also provides recommendations for policy and practice related to teacher education programmes.

Keywords: STEP, teacher education, Pakistan, Canada, Aga Khan foundation

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Authors: Shiraz A. Markarian

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Our systematic studies of diethylsulfoxide (DESO), the nearest homologue of dimethylsulfoxide (DMSO), reveal new physicochemical features. DESO has already received worthy biomedical applications: in some cases even are more pronounced compare with DMSO. The several important physicochemical characteristics of DESO including aqueous solutions have been verified and first reported: melting point of pure substance, density, dielectric relaxation data, vapor pressure and volumetric properties. Analysis of the complete vibrational spectra also leads to the conclusion that very strong interactions take place between DESO and water, even stronger than those between DMSO and water. The simultaneous existence of strong DESO-H₂O and DESO-DESO interactions suggest the coexistence of many types of structural molecular aggregates, the presence of which plays a significant role also in diluted water solutions. Our recent investigations have shown that aqueous solution of DESO could provide amorphous, glassy systems, thus avoiding ice crystallization, in a wide range of concentrations and even at very low cooling rates. The ability of DESO to act as an effective cryoprotectant on E. coli survival was also studied and compared with other commonly used cryoprotective agents. The results also confirm that DESO, more than DMSO, is able to penetrate living tissues without causing significant damage.

Keywords: diethylsulfoxide, dimethylsulfoxide, cryoprotectant, properties

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Authors: John Olayinka Atoyebi

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Developing countries like Nigeria are facing myriad problems, ranging from economic challenges, lack of no jobs, food insecurity, malnutrition, and poverty. However, tackling some of these menaces is not just a trivial issue neither do some of them require rocket science to fix, but rather the understanding of every individual citizen recognizing their respective roles that they have to play in making the country better, rather than putting all the blames on the Government. Tackling nutrition and food insecurity is a complex problem, but this work examines what an individual can do to improve nutrient consumption. Leafy indigenous vegetables can be termed as functional foods since they are very rich in nutrients, phytochemicals and other beneficial compounds to the body system. These functional foods are the class that provides necessary health benefits beyond basic nutrition. Usually functional foods often contain bioactive compounds, which help the body through the prevention and management of various diseases, as well as improving the overall health of human beings. The analysis carried out on some Nigerian leafy indigenous vegetables in home grown setting revealed, for example, the potential use of Iron (Fe) amount of 318.15ppm in Basella alba (red species) and that of Telfaria Occidentalis (Ugu) with 261.22ppm as being useful to stimulate heme, a necessary precursor and protein in the formation of blood in human being. Moreso, Virnonia amygdalina (ewuro) and water leaf possess anti-bacterial and anti-diabetic properties. They also provide digestive health benefits and support to the body system, including anti-inflammatory properties. Also, medicinal plant like Morinda citrifolia (Noni), which had been found to possess anti-cancer properties, has a Vitamin C amount of 528.85 mg/100g and a total carotenoids amount of 85.50 µg/g. However, despite all these results and potential utilization of these and other indigenous vegetables in Nigeria, there is a gross unawareness and/or non-cognizance of their utilization potentials, as some home garden lacks understanding of the immense nutrition benefits, thus hindering some of the populace to make proper use of these vegetables to enhance their health.

Keywords: developing countries, optimising, leafy vegetables, functional foods

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Authors: Ahmed Nouasri, Tahar Dob, Toumi Mohamed, Dahmane Dahmane, Soumioa Krimat, Lynda Lamari, Chabane Chelghom

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The aim of this study is to investigate the chemical composition for the first time, and antimicrobial activities of essential oil (EO) of Thymus lanceolatus Desf., an endemic thyme from Tiaret province of Algeria. The chemical composition of hydrodistilled essential oil from flowering aerial parts has been analyzed by GC and GC/MS techniques, the antimicrobial activity was realised by agar disc diffusion method and MIC was determined in solid medium by direct contact. Essential oil of T. lanceolataus has been yielded of 2.336 (w/w) based on dry weight, the analyses cited above, led to the identification of 29 components, which accounted for 97.34% of the total oil. Oxygenated monoterpenes was the main fraction (88.31%) dominated by thymol (80.2%) as major component of this oil, followed by carvacrol (6.25%). The oil was found effective against all tested strains especially fungus, except Pseudomonas aeruginosa were low activity observed, in addition Gram (+) bacteria found to be more sensitive to the EO than Gram (-) bacteria. This activity was ranging from12±2.65mm to 60.00±0.00mm Ø, with the lowest MIC value of under 0.06mg/ml to 12.53mg/ml. This results provided the evidence that the studied plant might indeed be potential sources of natural antimicrobial agents

Keywords: Thymus lanceolatus Desf., essential oil, chemical composition, antimicrobial activities

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Authors: Jana Tchekalarova, Stela Georgieva, Petia Peneva, Petar Todorov

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In the present study, a series of bioconjugates of N-modified hemorphine analogs containing second pharmacophore cinnamic acids (CA) or caffeic acid (KA) were synthesized by a traditional solid-phase Fmoc chemistry method for peptide synthesis. Electrochemical and fluorometric analysis and in vivo anticonvulsant activity in mice were conducted on the compounds. The three CA (H4-CA, H5-CA, and H7-CA) and three KA (H4-KA, H5-KA, and H7-KA)-conjugated hemorphine derivatives showed dose-dependent anticonvulsant activity in the maximal electroshock test (MES) in mice. The KA-conjugated H5-KA derivate was the only compound that suppressed clonic seizures at the lowest dose of 0.5 µg/mouse in the scPTZ test. The activity against the psychomotor seizures in the 6-Hz test was detected only for the H4-CA (0.5 µg) and H4-KA (0.5 µg and 1 µg), respectively. The peptide derivates did not exhibit neurotoxicity in the rotarod test. Our findings suggest that conjugated CA and KA hemorphine peptides can be used as a background for developing hemorphin-related analogs with anticonvulsant activity. Acknowledgments: This study is funded by the European Union-NextGenerationEU, through the National Recovery and Resilience Plan of the Republic of Bulgaria, project № BG-RRP-2.004-0002, "BiOrgaMCT".

Keywords: hemorphins, SPSS, caffeic/cinnamic acid, anticonvulsant activity, electrochemistry, fluorimetry

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Authors: Ihcen Khacheba, Amar Djeridane, Abdelkarim Kamli, Mohamed Yousfi

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Plant materials constitute an important source of natural bioactive molecules. Thus plants have been used from antiquity as sources of medicament against various diseases. These properties are usually attributed to secondary metabolites that are the subject of a lot of research in this field. This is particularly the case of phenolic compounds plants that are widely renowned in therapeutics as anti-inflammatories, enzyme inhibitors, and antioxidants, particularly flavonoïds. With the aim of acquiring a better knowledge of the secondary metabolism of the vegetable kingdom in the region of Laghouat and of the discovering of new natural therapeutics, 10 extracts from 5 Saharan plant species were submitted to chemical screening.The analysis of the preceding biological targets led to the evaluation of the biological activity of the extracts of the species Genista Corsica. The first step, consists in extracting and quantifying phenolic compounds. The second step has been devoted to stugying the effects of phenolic compounds on the kinetics catalyzed by two enzymes belonging to the class of hydrolase (the α-amylase and α-glucosidase) responsible for the digestion of sugars and finally we evaluate the antiantioxidant potential. The analysis results of phenolic extracts show clearly a low content of phenolic compounds in investigated plants. Average total phenolics ranged from 0.0017 to 11.35 mg equivalent gallic acid/g of the crude extract. Whereas the total flavonoids content lie between 0.0015 and 10.,96 mg/g equivalent of rutin. The results of the kinetic study of enzymatic reactions show that the extracts have inhibitory effects on both enzymes, with IC50 values ranging from 95.03 µg/ml to 1033.53 µg/ml for the α-amylase and 279.99 µg/ml to 1215.43 µg/ml for α-glucosidase whose greatest inhibition was found for the acetone extract of June (IC50 = 95.03 µg/ml). The results the antioxidant activity determined by ABTS, DPPH, and phosphomolybdenum tests clearly showed a good antioxidant capacity comparatively to antioxidants taken as reference the biological potential of these plants and could find their use in medicine to replace synthetic products.

Keywords: phenolic extracts, inhibition effect, α-amylase, α-glucosidase, antioxidant activity

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Authors: Mahdokht Sadeghvishkaei, Azizah Abdul-Hamid, Amin Ismail, Nazamid Saari

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Hypertension is a common and serious chronic health problem and known as the most important risk factor for development of many diseases such as stroke. Since angiotensin I-converting enzyme (ACE) is the key enzyme involved in blood pressure, one of the well accepted mechanisms to control hypertension is through ACE inhibition. The ACE inhibitory effect of Actinopyga lecanora (stone fish) proteolysate in vitro had been reported. Hence, this study aimed to evaluate the ACE inhibitory potential of Actinopyga lecanora proteolysate in vivo in normotensive rats. Therefore the ACE inhibitory capability of the proteolysate to prevent increasing systolic blood pressure, after inducing hypertension by angiotensin I was examined. The pre-fed rats with the proteolysates at various doses (200, 400, 800 mg/kg body weight) revealed the significant (p ≤ 0.05) suppression effect compared with control groups. Furthermore, different doses of the proteolysate (200, 400, 800 mg/kg body weight) were examined to find its optimum effective dose. Results depicted that 800 mg proteolysate/kg body weight significantly reduced systolic blood pressure without negative effect on normal blood pressure (p ≤ 0.05). Furthermore, Sub-acute toxicity study based on OECD guideline demonstrated the safety of the proteolysate in vivo. The present study indicated that the proteolysate at a dose of 1000 mg/kg daily for 14 days did not cause toxicity signs such as death, changes in activity, or piloerection. Since there are no significant differences between treated groups and control groups, hematological and biochemical analysis confirmed safety of the proteolysate (p > 0.05). In addition, there were no significant differences between organs weights of the treated groups and the control groups. Morphologically, neither histopathological changes, nor gross abnormalities were observed. However, the proteolysate caused significant decrease in body weight in relation to the control groups (p ≤ 0.05) probably due to appetite stimulation by the proteolysate, leading to decreased food consumption in sub-acute group. It is concluded that the proteolysate generated from Actinopyga lecanora possess a significant anti-hypertensive effect and would be potentially used as natural alternative of ACE inhibitors.

Keywords: ACE inhibition, Actinopyga lecanora, anti-hypertensive activity, bioactive peptides, normotensive rats

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Authors: Ana Fonseca, Ana Gouveia, Edgar Ramalho, Rita Henriques, Filipa Figueiredo, João Nunes

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Due to persistent climate pressures, there is a need to find a resilient economic system that is regenerative in nature. Bioeconomy offers the possibility of replacing non-renewable and non-biodegradable materials derived from fossil fuels with ones that are renewable and biodegradable, while a Circular Economy aims at sustainable and resource-efficient operations. The term "Circular Bioeconomy", which can be summarized as all activities that transform biomass for its use in various product streams, expresses the interaction between these two ideas. Portugal has a very favourable context to promote a Circular Bioeconomy due to its variety of climates and ecosystems, availability of biologically based resources, location, and geomorphology. Recently, there have been political and legislative efforts to develop the Portuguese Circular Bioeconomy. The Action Plan for a Sustainable Bioeconomy, approved in 2021, is composed of five axes of intervention, ranging from sustainable production and the use of regionally based biological resources to the development of a circular and sustainable bioindustry through research and innovation. However, as some statistics show, Portugal is still far from achieving circularity. According to Eurostat, Portugal has circularity rates of 2.8%, which is the second lowest among the member states of the European Union. Some challenges contribute to this scenario, including sectorial heterogeneity and fragmentation, prevalence of small producers, lack of attractiveness for younger generations, and absence of implementation of collaborative solutions amongst producers and along value chains.Regarding the Portuguese industrial sector, there is a tendency towards complex bureaucratic processes, which leads to economic and financial obstacles and an unclear national strategy. Together with the limited number of incentives the country has to offer to those that pretend to abandon the linear economic model, many entrepreneurs are hesitant to invest the capital needed to make their companies more circular. Absence of disaggregated, georeferenced, and reliable information regarding the actual availability of biological resources is also a major issue. Low literacy on bioeconomy among many of the sectoral agents and in society in general directly impacts the decisions of production and final consumption. The WinBio project seeks to outline a strategic approach for the management of weaknesses/opportunities in the technology transfer process, given the reality of the territory, through road mapping and national and international benchmarking. The developed work included the identification and analysis of agents in the interior region of Portugal, natural endogenous resources, products, and processes associated with potential development. Specific flow of biological wastes, possible value chains, and the potential for replacing critical raw materials with bio-based products was accessed, taking into consideration other countries with a matured bioeconomy. The study found food industry, agriculture, forestry, and fisheries generate huge amounts of waste streams, which in turn provide an opportunity for the establishment of local bio-industries powered by this biomass. The project identified biological resources with potential for replication and applicability in the Portuguese context. The richness of natural resources and potentials known in the interior region of Portugal is a major key to developing the Circular Economy and sustainability of the country.

Keywords: circular bioeconomy, interior region of portugal, regional development., public policy

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Authors: Olufemi Oyedele

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Building collapse (BC) in Nigeria is becoming a regular occurrence, each recording great casualties in the number of lives and materials lost. Building collapse is a situation where building which has been completed and occupied, completed but not occupied or under construction, collapses on its own due to action or inaction of man or due to natural event like earthquake, storm, flooding, tsunami or wildfire. It is different from building demolition. There are various causes of building collapse and each case requires expert judgment to decide the cause of its collapse. Rate of building collapse is a reflection of the level of organization and control of building activities and degree of sophistication of the construction professionals in a country. This study explored the use of case study by examining the causes of six (6) collapsed buildings (CB) across Nigeria. Samples of materials from the sites of the collapsed buildings were taken for testing and analysis, while critical observations were made at the sites to note the conditions of the ground (building base). The study found out that majority of the building collapses in Nigeria were due to poor workmanship, sub-standard building materials, followed by bad building base and poor design. The National Building Code 2006 is not effective due to lack of enforcement and the Physical Development Departments of states and Federal Capital Territory are just mere agents of corruption allowing all types of construction without building approvals.

Keywords: building collapse, concrete tests, differential settlement, integrity test, quality control

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Authors: Parastoo Motallebi, Vahid Niknam, Hassan Ebrahimzadeh, Majid Hashemi

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Wheat, the most strategically important worldwide crop, is widely grown in various countries. Based on international wheat production statistics (FAOSTAT database), the total production of wheat in 2012 was 13.8 in Iran. Fusarium culmorum is one of the principal causative agents of Fusarium crown rot (FCR), an overwhelming disease of wheat and barley which is in the early stages causing yield losses, stand reductions and rotting of root and lower stem tissues. In this study inoculation of two wheat seedlings of the susceptible cultivar Falat and the partially field-resistant cultivar Pishtaz were carried out in greenhouse conditions and root samples were taken for 6 days. The activity of peroxidase (POX) and polyphenoloxidase (PPO) enzymes were analyzed to identify possible relations between resistance and enzymatic activities. Although the POX and PPO activities in both geno types increased, this significant increase was more dominant in Pishtaz. The results showed an earlier elevation in the activity of these defense related enzymes in semi-resistant cv. Pishtaz after inoculation, suggested that the activities of POX and PPO in wheat geno types play an important role in the induction of resistance to this disease.

Keywords: Defense responses, Fusarium culmorum, Wheat

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