Search results for: Molecular modeling of 17-picolyl and 17-picolinylidene androstane derivatives with anticancer activity

Authors: Narasamma Nippatlapallia

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Communities across the world are desperate to get their environment free of toxic per-poly fluoroalkyl substances (PFAS) especially when these chemicals are in aqueous media. In the present study, two different chain length PFAS (PFHxA (C6), PFDA (C10)) are selected for degradation using a modified continuous flow nonthermal plasma. The results showed 82.3% PFHxA and 94.1 PFDA degradation efficiencies, respectively. The defluorination efficiency is also evaluated which is 28% and 34% for PFHxA and PFDA, respectively. The results clearly indicates that the structure of PFAS has a great impact on degradation efficiency. The effect of flow rate is studied. increase in flow rate beyond 2 mL/min, decrease in degradation efficiency of the targeted PFAS was noticed. PFDA degradation was decreased from 85% to 42%, and PFHxA was decreased to 32% from 64% with increase in flow rate from 2 to 5 mL/min. Similarly, with increase in flow rate the percentage defluorination was decreased for both C10, and C6 compounds. This observation can be attributed to mainly because of change in residence time (contact time). Real water/wastewater is a composition of various organic, and inorganic ions that may affect the activity of oxidative species such as 𝑂𝐻. radicals on the target pollutants. Therefore, it is important to consider radicals quenching chemicals to understand the efficiency of the reactor. In gas-liquid NTP discharge reactors 𝑂𝐻. , 𝑒𝑎𝑞 − , 𝑂 . , 𝑂3, 𝐻2𝑂2, 𝐻. are often considered as reactive species for oxidation and reduction of pollutants. In this work, the role played by two distinct 𝑂 .𝐻 Scavengers, ethanol and glycerol, on PFAS percentage degradation, and defluorination efficiency (i,e., fluorine removal) are measured was studied. The addition of scavenging agents to the PFAS solution diminished the PFAS degradation to different extents depending on the target compound molecular structure. In comparison with the degradation of only PFAS solution, the addition of 1.25 M ethanol inhibited C10, and C6 degradation by 8%, and 12%, respectively. This research was supported with energy efficiency, production rate, and specific yield, fluoride, and PFAS concentration analysis with respect to optimum hydraulic retention time (HRT) of the continuous flow reactor.

Keywords: wastewater, PFAS, nonthermal plasma, mineralization, defluorination

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Authors: L. Grinis

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Turbulent flow in complex geometries receives considerable attention due to its importance in many engineering applications. It has been the subject of interest for many researchers. Some of these interests include the design of storm water channels. The design of these channels requires testing through physical models. The main practical limitation of physical models is the so called “scale effect”, that is, the fact that in many cases only primary physical mechanisms can be correctly represented, while secondary mechanisms are often distorted. These observations form the basis of our study, which centered on problems associated with the design of storm water channels near the Dead Sea, in Israel. To help reach a final design decision we used different physical models. Our research showed good coincidence with the results of laboratory tests and theoretical calculations, and allowed us to study different effects of fluid flow in an open channel. We determined that problems of this nature cannot be solved only by means of theoretical calculation and computer simulation. This study demonstrates the use of physical models to help resolve very complicated problems of fluid flow through baffles and similar structures. The study applies these models and observations to different construction and multiphase water flows, among them, those that include sand and stone particles, a significant attempt to bring to the testing laboratory a closer association with reality.

Keywords: open channel, physical modeling, baffles, turbulent flow

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Authors: Kalaumari Mayoral-Peña, Ana I. Montejano-Montelongo, Josué Reyes-Muñoz, Gonzalo A. Ortiz-Mancilla, Mayrin Rodríguez-Cruz, Víctor Hernández-Villalobos, Jesús A. Guzmán-López, Santiago García-Jacobo, Iván Licona-Vázquez, Grisel Fierros-Romero, Rosario Flores-Vallejo

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The group B-lactamic antibiotics include some of the most frequently used small drug molecules against bacterial infections. Nevertheless, an alarming decrease in their efficacy has been reported due to the emergence of antibiotic-resistant bacteria. Infections caused by bacteria expressing extended Spectrum B-lactamases (ESBLs) are difficult to treat and account for higher morbidity and mortality rates, delayed recovery, and high economic burden. According to the Global Report on Antimicrobial Resistance Surveillance, it is estimated that mortality due to resistant bacteria will ascend to 10 million cases per year worldwide. These facts highlight the importance of developing low-cost and readily accessible detection methods of drug-resistant ESBLs bacteria to prevent their spread and promote accurate and fast diagnosis. Bacterial detection is commonly done using molecular diagnostic techniques, where PCR stands out for its high performance. However, this technique requires specialized equipment not available everywhere, is time-consuming, and has a high cost. Loop-Mediated Isothermal Amplification (LAMP) is an alternative technique that works at a constant temperature, significantly decreasing the equipment cost. It yields double-stranded DNA of several lengths with repetitions of the target DNA sequence as a product. Although positive and negative results from LAMP can be discriminated by colorimetry, fluorescence, and turbidity, there is still a large room for improvement in the point-of-care implementation. DNA origami is a technique that allows the formation of 3D nanometric structures by folding a large single-stranded DNA (scaffold) into a determined shape with the help of short DNA sequences (staples), which hybridize with the scaffold. This research aimed to generate DNA origami structures using LAMP products as scaffolds to improve the sensitivity to detect ESBLs in point-of-care diagnosis. For this study, the coding sequence of the CTM-X-15 ESBL of E. coli was used to generate the LAMP products. The set of LAMP primers were designed using PrimerExplorerV5. As a result, a target sequence of 200 nucleotides from CTM-X-15 ESBL was obtained. Afterward, eight different DNA origami structures were designed using the target sequence in the SDCadnano and analyzed with CanDo to evaluate the stability of the 3D structures. The designs were constructed minimizing the total number of staples to reduce costs and complexity for point-of-care applications. After analyzing the DNA origami designs, two structures were selected. The first one was a zig-zag flat structure, while the second one was a wall-like shape. Given the sequence repetitions in the scaffold sequence, both were able to be assembled with only 6 different staples each one, ranging between 18 to 80 nucleotides. Simulations of both structures were performed using scaffolds of different sizes yielding stable structures in all the cases. The generation of the LAMP products were tested by colorimetry and electrophoresis. The formation of the DNA structures was analyzed using electrophoresis and colorimetry. The modeling of novel detection methods through bioinformatics tools allows reliable control and prediction of results. To our knowledge, this is the first study that uses LAMP products and DNA-origami in combination to delect ESBL-producing bacterial strains, which represent a promising methodology for diagnosis in the point-of-care.

Keywords: beta-lactamases, antibiotic resistance, DNA origami, isothermal amplification, LAMP technique, molecular diagnosis

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Authors: Dena Alhaloul

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The Middle East and North Africa (MENA) region is characterized by diverse cultures, economies, and social structures. Fertility rates in MENA have seen significant changes over time, with variations among countries and subregions. Understanding fertility patterns in this region is essential due to its impact on demographic dynamics, healthcare, labor markets, and social policies. Rising or declining fertility rates have far-reaching consequences for the region's socioeconomic development. The main thrust of this study is to comprehensively examine fertility rates in the Middle East and North Africa (MENA) region. It aims to understand the distribution, determinants, and temporal trends of fertility rates in MENA countries. The study seeks to provide insights into the factors influencing fertility decisions, assess how fertility rates have evolved over time, and potentially develop statistical models to characterize these trends. As for the methodology of the study, the study uses descriptive statistics to summarize and visualize fertility rate data. It also uses regression analyses to identify determinants of fertility rates as well as statistical modeling to characterize temporal trends in fertility rates. The conclusion of this study The research will contribute to a deeper understanding of fertility dynamics in the MENA region, shedding light on the distribution of fertility rates, their determinants, and historical trends.

Keywords: fertility, distribution, modeling, regression

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Authors: Wen-Jay Lee, Kuo-Ning Chiang

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The graphene binding with silicon substrate has apparently Schottky barriers property, which can be used in the application of solar cell and light source. Because graphene has only one atom layer, the atomistic structure of graphene binding with the silicon surface plays an important role to affect the properties of graphene. In this work, temperature effect on the morphology of graphene sheet attached on different crystal planes of silicon substrates are investigated by Molecular dynamics (MD) (LAMMPS, developed by Sandia National Laboratories). The results show that the covered graphene sheet would cause the structural deformation of the surface Si atoms of stubtrate. To achieve a stable state in the binding process, the surface Si atoms would adjust their position and fit the honeycomb structure of graphene after the graphene attaches to the Si surface. The height contour of graphene on different plane of silicon surfaces presents different pattern, leading the local residual stress at the interface. Due to the high density of dangling bond on the Si (111)7x7 surface, the surface of Si(111)7x7 is not matching with the graphene so well in contrast with Si(100)2x1and Si(111)2x1. Si(111)7x7 is found that only partial silicon adatoms are rearranged on surface after the attachment when the temperature is lower than 200K, As the temperature gradually increases, the deformation of surface structure becomes significant, as well as the residue stress. With increasing temperature till the 815K, the graphene sheet begins to destroy and mixes with the silicon atoms. For the Si(100)2x1 and Si(111)2x1, the silicon surface structure keep its structural arrangement with a higher temperature. With increasing temperature, the residual stress gradually decrease till a critical temperatures. When the temperature is higher than the critical temperature, the residual stress gradually increases and the structural deformation is found on the surface of the Si substrates.

Keywords: molecular dynamics, graphene, silicon, Schottky barriers, interface

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Authors: Sara Przetocka, Krzysztof Żak, Grzegorz Dubin, Tadeusz Holak

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Toll-like receptors (TLRs) play central role in the innate immune response and inflammation by recognizing pathogen-associated molecular patterns (PAMPs). A fundamental basis of TLR signalling is dependent upon the recruitment and association of adaptor molecules that contain the structurally conserved Toll/interleukin-1 receptor (TIR) domain. MyD88 (myeloid differentiation primary response gene 88) is the universal adaptor for TLRs and cooperates with Mal (MyD88 adapter-like protein, also known as TIRAP) in TLR4 response which is predominantly used in inflammation, host defence and carcinogenesis. Up to date two possible models of MyD88, Mal and TLR4 interactions have been proposed. The aim of our studies is to confirm or abolish presented models and accomplish the full structural characterisation of TIR domains interaction. Using molecular cloning methods we obtained several construct of MyD88 and Mal TIR domain with GST or 6xHis tag. Gel filtration method as well as pull-down analysis confirmed that recombinant TIR domains from MyD88 and Mal are binding in complexes. To examine whether obtained complexes are homo- or heterodimers we carried out cross-linking reaction of TIR domains with BS3 compound combined with mass spectrometry. To investigate which amino acid residues are involved in this interaction the NMR titration experiments were performed. 15N MyD88-TIR solution was complemented with non-labelled Mal-TIR. The results undoubtedly indicate that MyD88-TIR interact with Mal-TIR. Moreover 2D spectra demonstrated that simultaneously Mal-TIR self-dimerization occurs which is necessary to create proper scaffold for Mal-TIR and MyD88-TIR interaction. Final step of this study will be crystallization of MyD88 and Mal TIR domains complex. This crystal structure and characterisation of its interface will have an impact in understanding the TLR signalling pathway and possibly will be used in development of new anti-cancer treatment.

Keywords: cancer, MyD88, TIR domains, Toll-like receptors

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Authors: Armando A. Rodríguez, Emilio Salceda, Anoland Garateix, André J. Zaharenko, Steve Peigneur, Omar López, Tirso Pons, Michael Richardson, Maylín Díaz, Yasnay Hernández, Ludger Ständker, Jan Tytgat, Enrique Soto

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Acid-sensing ion channels are cation (Na+) channels activated by a pH drop. These proteins belong to the ENaC/degenerin superfamily of sodium channels. ASICs are involved in sensory perception, synaptic plasticity, learning, memory formation, cell migration and proliferation, nociception, and neurodegenerative disorders, among other processes; therefore those molecules that specifically target these channels are of growing pharmacological and biomedical interest. Sea anemones produce a large variety of ion channels peptide toxins; however, those acting on ligand-gated ion channels, such as Glu-gated, Ach-gated ion channels, and acid-sensing ion channels (ASICs), remain barely explored. The peptide PhcrTx1 is the first compound characterized from the sea anemone Phymanthus crucifer, and it constitutes a novel ASIC inhibitor. This peptide was purified by chromatographic techniques and pharmacologically characterized on acid-sensing ion channels of mammalian neurons using patch-clamp techniques. PhcrTx1 inhibited ASIC currents with an IC50 of 100 nM. Edman degradation yielded a sequence of 32 amino acids residues, with a molecular mass of 3477 Da by MALDI-TOF. No similarity to known sea anemone peptides was found in protein databases. The computational analysis of Cys-pattern and secondary structure arrangement suggested that this is a structurally ICK (Inhibitor Cystine Knot)-type peptide, a scaffold that had not been found in sea anemones but in other venomous organisms. These results show that PhcrTx1 represents the first member of a new structural group of sea anemones toxins acting on ASICs. Also, this peptide constitutes a novel template for the development of drugs against pathologies related to ASICs function.

Keywords: animal toxin, inhibitor cystine knot, ion channel, sea anemone

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Authors: M. A. Ferhat, M. N. Boukhatem, F. Chemat

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Since the available anti-inflammatory drugs exert an extensive variety of side effects, the search for new anti-inflammatory agents has been a priority of pharmaceutical industries. The aim of the present study was to assess the anti-inflammatory activities of the essential oil of rose geranium (RGEO). The chemical composition of the RGEO was investigated by gas chromatography. The major components were citronellol (29.13%), geraniol (12.62%), and citronellyl formate (8.06%). In the carrageenan induced paw edema, five different groups were established and RGEO was administered orally in three different doses. RGEO (100 mg/kg) was able to significantly reduce the paw edema with a comparable effect to that observed with diclofenac, the positive control. In addition, RGEO showed a potent anti-inflammatory activity by topical treatment in the method of croton oil-induced ear edema. When the dose was 5 or 10 ml of RGEO per ear, the inflammation was reduced by 73 and 88%, respectively. This is the first report to demonstrate a significant anti-inflammatory activity of Algerian RGEO. In addition, histological analysis confirmed that RGEO inhibited the inflammatory responses in the skin. Our results indicate that RGEO may have significant potential for the development of novel anti-inflammatory drugs with improved safety profile.

Keywords: anti-inflammatory effect, carrageenan, citronellol, histopathology, Rose geranium

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Authors: Abrar Al-Mutairi, Talal Al-Bazali

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In this study, changes in capillary entry pressure of shale, as it interacts with CO₂, under different temperatures (25 °C to 250 °C) have been investigated. The combined impact of temperature and petrophysical properties (water content, water activity, permeability and porosity) of shale was also addressed. Results showed that the capillary entry pressure of shale when it interacted with CO₂ was highly affected by temperature. In general, increasing the temperature decreased capillary entry pressure of shale. We believe that pore dilation, where pore throat size expands due to the application of heat, may have caused this decrease in capillary entry pressure of shale. However, in some cases we found that at higher temperature some shale samples showed that the temperature activated clay swelling may have caused an apparent decrease in pore throat radii of shale which translates into higher capillary entry pressure of shale. Also, our results showed that there is no distinct relationship between shale’s water content, water activity, permeability, and porosity on the capillary entry pressure of shale samples as it interacted with CO₂ at different temperatures.

Keywords: heat, threshold pressure, CO₂ sequestration, shale

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Authors: Bayan Alqassem, Israa A. Othman, Mohammed Abu Haija, Fawzi Banat

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The treatment of wastewater from highly toxic pollutants is one of the most challenging issues for humanity. In this study, the advanced oxidation process (AOP) was employed to study the catalytic degradation of phenol using different ferrite catalysts which are CoFe₂O₄, CrFe₂O₄, CuFe₂O₄, MgFe₂O₄, MnFe₂O₄, NiFe₂O₄ and ZnFe₂O₄. The ferrite catalysts were prepared via sol-gel and co-precipitation methods. Different ferrite composites were also prepared either by varying the metal ratios or incorporating chemically reduced graphene oxide in the ferrite cluster. The effect of phosphoric acid treatment on the copper ferrite activity. All of the prepared catalysts were characterized using infrared spectroscopy (IR), X-ray diffraction (XRD) and scanning electron microscopy (SEM). The ferrites catalytic activities were tested towards phenol degradation using high performance liquid chromatography (HPLC). The experimental results showed that ferrites prepared through sol-gel route were more active than those of the co-precipitation method towards phenol degradation. In both cases, CuFe₂O₄ exhibited the highest degradation of phenol compared to the other ferrites. The photocatalytic properties of the ferrites were also investigated.

Keywords: ferrite catalyst, ferrite composites, phenol degradation, photocatalysis

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Authors: Han Xiao

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The development of nanomedicines has recently achieved several breakthroughs in the field of cancer treatment; however, the biocompatibility and targeted burst release of these medications remain a limitation, which leads to serious side effects and significantly narrows the scope of their applications. The self-assembly of intermediate filament protein (IFP) peptides was triggered by a hydrophobic cation drug 7-amino actinomycin D (7-AAD) to synthesize pH-activatable nanoparticles (NPs) that could simultaneously locate tumors and produce antitumor effects. The designed IFP peptide included a target peptide (arginine–glycine–aspartate), a negatively charged region, and an α-helix sequence. It also possessed the ability to encapsulate 7-AAD molecules through the formation of hydrogen bonds and hydrophobic interactions by a one-step method. 7-AAD molecules with excellent near-infrared fluorescence properties could be target delivered into tumor cells by NPs and released immediately in the acidic environments of tumors and endosome/lysosomes, ultimately inducing cytotoxicity by arresting the tumor cell cycle with inserted DNA. It is noteworthy that the IFP/7-AAD NPs tail vein injection approach demonstrated not only high tumor-targeted imaging potential, but also strong antitumor therapeutic effects in vivo. The proposed strategy may be used in the delivery of cationic antitumor drugs for precise imaging and cancer therapy.

Keywords: 7-amino actinomycin D, intermediate filament protein, nanoparticle, tumor image

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Authors: Abhishek Ranka

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Rock-cut Architecture is a manifestation of human endurance in constructing magnificent structures by sculpting and cutting entire hills. Cave Architecture in India form an important part of rock-cut development and is among the most prolific examples of rock-cut architecture in the world. There are more than 1500 rock-cut caves in various regions of India. Among them mostly are located in western India, more particularly in the state of Maharashtra. Some of the rock-cut caves are located in the central region of India, which is presently known as Malawa (Madhya Pradesh). The region is dominated by the vidhyachal hill ranges toward the west, dotted with the coarse laterite rock. Dhamnar Caves have been excavated in the central region of Mandsaur Dist. With a combination of shared sacred faiths. The earliest rock-cut activity began in the north, in Bihar, where caves were excavated in the Barabar and the Nagarjuni hills during the Mauryan period (3rd century BCE). The rock-cut activity then shifts to the central part of India in Madhya Pradesh, where the caves at Dhamnar, Bagh, Udayagiri, Poldungar, etc. excavated between 3rdto 9ᵗʰ CE. The rock-cut excavation continued to flourish in Madhya Pradesh till 10ᵗʰ century CE, simultaneously with monolithic Hindu temples. Dhamnar caves fall into four architectural typologies: the Lena caves, Chaitya caves, Viharas & Lena-Chaityagriha caves. The Buddhist rock-cutting activity in central India is divisible into two phases. In the first phase (2ndBCE-3rd CE), the Buddha image is conspicuously absent. After a lapse of about three centuries, activity begins again, and the Buddha images this time are carved. The former group belongs to the Hinayana (Lesser Vehicle) phase and the latter to the Mahayana (Greater Vehicle). Dhamnar caves has an elaborate facades, pillar capitals, and many more creative sculptures in various postures. These caves were excavated against the background of invigorating trade activities and varied socio-religious or Socio Cultural contexts. These caves also highlights the wealthy and varied patronage provided by the dynasties of the past. This paper speaks about the appraisal of the rock cut mechanisms, design strategies, and approaches while promoting a scope for further research in conservation practices. Rock-cut sites, with their physical setting and various functional spaces as a sustainable habitat for centuries, has a heritage footprint with a researchquotient.

Keywords: rock-cut architecture, buddhism, hinduism, Iconography, and architectural typologies, Jainism

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Authors: Magdalena B. Kaziuk, Waldemar Kosiba

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Background: In the XXI century we have to deal with the epidemic of obesity which is important risk factor for the cardiovascular and kidney diseases. Lipo proteins are directly involved in the atherosclerotic process. Non-high-density lipo protein (non-HDL) began following widespread recognition of its superiority over LDL as a measurement of vascular event risk. Non-HDL includes residual risk which persists in patients after achieved recommended level of LDL. Materials and Methods: The study covered 111 patients (52 females, 59 males, age 51,91±14 years), hospitalized on the intern department. Body composition was assessed using the bioimpendance method and anthropometric measurements. Physical activity data were collected during the interview. The nutritional status and the obesity type were determined with the Waist to Height Ratio and the Waist to Hip Ratio. A function of the kidney was evaluated by calculating the estimated glomerular filtration rate (eGFR) using MDRD formula. Non-HDL was calculated as a difference between concentration of the Total and HDL cholesterol. Results: 10% of patients were found to be underweight; 23.9 % had correct body weight; 15,08 % had overweight, while the remaining group had obesity: 51,02 %. People with the android shape have higher non-HDL cholesterol versus with the gynoid shape (p=0.003). The higher was non-HDL, the lower eGFR had studied subjects (p < 0.001). Significant correlation was found between high non-HDL and incorrect dietary habits in patients avoiding eating vegetables, fruits and having low physical activity (p < 0.005). Conclusions: Android type of figure raises the residual risk of the heart disease associated with higher levels of non-HDL. Increasing physical activity in these patients reduces the level of non-HDL. Non-HDL seems to be the best predictor among all cholesterol measures for the cardiovascular events and worsening eGFR.

Keywords: obesity, non-HDL cholesterol, glomerular filtration rate, lifestyle

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Authors: Jing Jiang, Wenhuan XU, Lei Zhang, Shiyi Zhang, Tongli Wang

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Climate data quality significantly affects the reliability of ecological modeling. In the Asia Pacific (AP) region, low-quality climate data hinders ecological modeling. ClimateAP, a software developed in 2017, generates high-quality climate data for the AP region, benefiting researchers in forestry and agriculture. However, its adoption remains limited. This study aims to confirm the validity of biologically relevant variable data generated by ClimateAP during the normal climate period through comparison with the currently available gridded data. Climate data from 2,366 weather stations were used to evaluate the prediction accuracy of ClimateAP in comparison with the commonly used gridded data from WorldClim1.4. Univariate regressions were applied to 48 monthly biologically relevant variables, and the relationship between the observational data and the predictions made by ClimateAP and WorldClim was evaluated using Adjusted R-Squared and Root Mean Squared Error (RMSE). Locations were categorized into mountainous and flat landforms, considering elevation, slope, ruggedness, and Topographic Position Index. Univariate regressions were then applied to all biologically relevant variables for each landform category. Random Forest (RF) models were implemented for the climatic niche modeling of Cunninghamia lanceolata. A comparative analysis of the prediction accuracies of RF models constructed with distinct climate data sources was conducted to evaluate their relative effectiveness. Biologically relevant variables were obtained from three unpublished Chinese meteorological datasets. ClimateAPv3.0 and WorldClim predictions were obtained from weather station coordinates and WorldClim1.4 rasters, respectively, for the normal climate period of 1961-1990. Occurrence data for Cunninghamia lanceolata came from integrated biodiversity databases with 3,745 unique points. ClimateAP explains a minimum of 94.74%, 97.77%, 96.89%, and 94.40% of monthly maximum, minimum, average temperature, and precipitation variances, respectively. It outperforms WorldClim in 37 biologically relevant variables with lower RMSE values. ClimateAP achieves higher R-squared values for the 12 monthly minimum temperature variables and consistently higher Adjusted R-squared values across all landforms for precipitation. ClimateAP's temperature data yields lower Adjusted R-squared values than gridded data in high-elevation, rugged, and mountainous areas but achieves higher values in mid-slope drainages, plains, open slopes, and upper slopes. Using ClimateAP improves the prediction accuracy of tree occurrence from 77.90% to 82.77%. The biologically relevant climate data produced by ClimateAP is validated based on evaluations using observations from weather stations. The use of ClimateAP leads to an improvement in data quality, especially in non-mountainous regions. The results also suggest that using biologically relevant variables generated by ClimateAP can slightly enhance climatic niche modeling for tree species, offering a better understanding of tree species adaptation and resilience compared to using gridded data.

Keywords: climate data validation, data quality, Asia pacific climate, climatic niche modeling, random forest models, tree species

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Authors: Nasreen Thebo, W. Shaikh, A. J. Laghari, P. Nangni

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Prunus dulcis (Almond) shell extract is demonstrated for its biomedical applications. Shell extract prepared by soxhlet method and further characterized by UV-Visible spectrophotometer, atomic absorption spectrophotometer (AAS), FTIR, GC-MS techniques. In this study, the antifungal activity of almond shell extract was observed against clinically isolated pathogenic fungi by strip method. The antioxidant potential of crude shell extract of was evaluated by using DPPH (2-2-diphenyl-1-picryhydrazyl) and radical scavenging system. The possibility of short term therapy was only 20 days. The total antioxidant activity varied from 94.38 to 95.49% and total phenolic content was found as 4.455 mg/gm in almond shell extract. Finally the results provide a great therapeutic potential against Tinea capitis infection of scalp. Included in this study of shell extract that show scientific evidence for clinical efficacy, as well as found to be more useful in the treatment of dermatologic disorders and without any doubt it can be recommended to be Patent.

Keywords: Tinea capitis, DPPH, FTIR, GC-MS therapeutic treatment

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Authors: S. V. Akulinichev, S. A. Chaushansky, V. I. Derzhiev

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High dose rate (HDR) brachytherapy is a method of contact radiotherapy, when a single sealed source with an activity of about 10 Ci is temporarily inserted in the tumor area. The isotopes Ir-192 and (much less) Co-60 are used as active material for such sources. The other type of brachytherapy, the low dose rate (LDR) brachytherapy, implies the insertion of many permanent sources (up to 200) of lower activity. The pulse dose rate (PDR) brachytherapy can be considered as a modification of HDR brachytherapy, when the single source is repeatedly introduced in the tumor region in a pulse regime during several hours. The PDR source activity is of the order of one Ci and the isotope Ir-192 is currently used for these sources. The PDR brachytherapy is well recommended for the treatment of several tumors since, according to oncologists, it combines the medical benefits of both HDR and LDR types of brachytherapy. One of the main problems for the PDR brachytherapy progress is the shielding of the treatment area since the longer stay of patients in a shielded canyon is not enough comfortable for them. The use of Yb-169 as an active source material is the way to resolve the shielding problem for PDR, as well as for HRD brachytherapy. The isotope Yb-169 has the average photon emission energy of 93 KeV and the half-life of 32 days. Compared to iridium and cobalt, this isotope has a significantly lower emission energy and therefore requires a much lighter shielding. Moreover, the absorption cross section of different materials has a strong Z-dependence in that photon energy range. For example, the dose distributions of iridium and ytterbium have a quite similar behavior in the water or in the body. But the heavier material as lead absorbs the ytterbium radiation much stronger than the iridium or cobalt radiation. For example, only 2 mm of lead layer is enough to reduce the ytterbium radiation by a couple of orders of magnitude but is not enough to protect from iridium radiation. We have created an original facility to produce the start stable isotope Yb-168 using the laser technology AVLIS. This facility allows to raise the Yb-168 concentration up to 50 % and consumes much less of electrical power than the alternative electromagnetic enrichment facilities. We also developed, in cooperation with the Institute of high pressure physics of RAS, a new technology for manufacturing high-density ceramic cores of ytterbium oxide. Ceramics density reaches the limit of the theoretical values: 9.1 g/cm3 for the cubic phase of ytterbium oxide and 10 g/cm3 for the monoclinic phase. Source cores from this ceramics have high mechanical characteristics and a glassy surface. The use of ceramics allows to increase the source activity with fixed external dimensions of sources.

Keywords: brachytherapy, high, pulse dose rates, radionuclides for therapy, ytterbium sources

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Authors: Aasaithambi Kalaiselvi, Michael Gabriel Paulraj, Ekambaram Nakkeeran

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Emergences of mosquito vector-borne diseases are considered as a perpetual problem globally in tropical countries. The outbreak of several diseases such as chikungunya, zika virus infection and dengue fever has created a massive threat towards the living population. Frequent usage of synthetic insecticides like Dichloro Diphenyl Trichloroethane (DDT) eventually had its adverse harmful effects on humans as well as the environment. Since there are no perennial vaccines, prevention, treatment or drugs available for these pathogenic vectors, WHO is more concerned in eradicating their breeding sites effectively without any side effects on humans and environment by approaching plant-derived natural eco-friendly bio-insecticides. The aim of this study is to investigate the larvicidal potency of Cinnamomum verum essential oil (CEO) loaded niosomes. Cholesterol and surfactant variants of Span 20, 60 and 80 were used in synthesizing CEO loaded niosomes using Transmembrane pH gradient method. The synthesized CEO loaded niosomes were characterized by Zeta potential, particle size, Fourier Transform Infrared Spectroscopy (FT-IR), GC-MS and SEM analysis to evaluate charge, size, functional properties, the composition of secondary metabolites and morphology. The Z-average size of the formed niosomes was 1870.84 nm and had good stability with zeta potential -85.3 meV. The entrapment efficiency of the CEO loaded niosomes was determined by UV-Visible Spectrophotometry. The bio-potency of CEO loaded niosomes was treated and assessed against gram-positive (Bacillus subtilis) and gram-negative (Escherichia coli) bacteria and fungi (Aspergillus fumigatus and Candida albicans) at various concentrations. The larvicidal activity was evaluated against II to IV instar larvae of Aedes aegypti, Anopheles stephensi and Culex quinquefasciatus at various concentrations for 24 h. The mortality rate of LC₅₀ and LC₉₀ values were calculated. The results exhibited that CEO loaded niosomes have greater efficiency against mosquito larvicidal activity. The results suggest that niosomes could be used in various applications of biotechnology and drug delivery systems with greater stability by altering the drug of interest.

Keywords: Cinnamomum verum, niosomes, entrapment efficiency, bactericidal and fungicidal, mosquito larvicidal activity

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Authors: Essia Sebai, Amel Abidi, Hayet benyeddem, Akkari Hafidh

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Herbal extracts are of particular interest to the drug industry; essential oil with significant anthelmintic activity has the potential to be used as an alternative to conventional chemical drugs. In the present study, we describe the chemical profile of Laurus nobilis essential oil (EO), the in vitro anthelmintic activity of laurel oil against Haemonchus contortus and its in vivo anthelmintic effect against the murine helminth parasite model Heligmosomoides polygyrus. The chromatographic profile of L. nobilis (EO) extracted from the leaves of L. nobilis has shown the presence of monoterpenes 1,8-cineol (Eucalyptol) (29.47%), D-Limonène (18.51%) and Linalool (10.84%) in high fractions. The in vitro anthelmintic potential was expressed by an ovicidal effect against H. contortus egg hatching with an inhibition value of 3.23 mg/mL and 87.5% of immobility of adult worms after 8 hours of exposure to 8 mg/mL of L. nobilis EO. Regarding the in vivo anthelmintic potential, L. nobilis (EO) at 2400 mg/kg completely eliminated the egg output of H. polygyrus after seven days of oral treatment, together with a 79.2% of reduction in total worm counts. Based on the obtained funding, L. nobilis EO showed promising in vitro and in vivo anthelmintic capacities against gastrointestinal parasites.

Keywords: lauris nobilis, anthelmintic, haemonchus, pylogyrus

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Authors: Yasuyuki Takahashi, Maya Yamashita, Kyoko Saito

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In general, dynamic SPECT data acquisition needs a few minutes for one rotation. Thus, the time-activity curve (TAC) derived from the dynamic SPECT is relatively coarse. In order to effectively shorten the interval, between data points, we adopted a 180-degree interpolation method. This method is already used for reconstruction of the X-ray CT data. In this study, we applied this 180-degree interpolation method to SPECT and investigated its effectiveness.To briefly describe the 180-degree interpolation method: the 180-degree data in the second half of one rotation are combined with the 180-degree data in the first half of the next rotation to generate a 360-degree data set appropriate for the time halfway between the first and second rotations. In both a phantom and a patient study, the data points from the interpolated images fell in good agreement with the data points tracking the accumulation of 99mTc activity over time for appropriate region of interest. We conclude that data derived from interpolated images improves the apparent time resolution of dynamic SPECT.

Keywords: dynamic SPECT, time resolution, 180-degree interpolation method, 99mTc-GSA.

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Authors: Kamlesh Shashikant Dave

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The global financial crisis is rooted in the sub-prime crisis in U.S.A. During the boom years, mortgage brokers attracted by the big commission, encouraged buyers with poor credit to accept housing mortgages with little or no down payment and without credit check. A combination of low interest rates and large inflow of foreign funds during the booming years helped the banks to create easy credit conditions for many years. Banks lent money on the assumptions that housing price would continue to rise. Also the real estate bubble encouraged the demand for houses as financial assets .Banks and financial institutions later repackaged these debts with other high risk debts and sold them to worldwide investors creating financial instruments called collateral debt obligations (CDOs). With the rise in interest rate, mortgage payments rose and defaults among the subprime category of borrowers increased accordingly. Through the securitization of mortgage payments, a recession developed in the housing sector and consequently it was transmitted to the entire US economy and rest of the world. The financial credit crisis has moved the US and the global economy into recession. Indian economy has also affected by the spill over effects of the global financial crisis. Great saving habit among people, strong fundamentals, strong conservative and regulatory regime have saved Indian economy from going out of gear, though significant parts of the economy have slowed down. Industrial activity, particularly in the manufacturing and infrastructure sectors decelerated. The service sector too, slow in construction, transport, trade, communication, hotels and restaurants sub sectors. The financial crisis has some adverse impact on the IT sector. Exports had declined in absolute terms in October. Higher inputs costs and dampened demand have dented corporate margins while the uncertainty surrounding the crisis has affected business confidence. To summarize, reckless subprime lending, loose monetary policy of US, expansion of financial derivatives beyond acceptable norms and greed of Wall Street has led to this exceptional global financial and economic crisis. Thus, the global credit crisis of 2008 highlights the need to redesign both the global and domestic financial regulatory systems not only to properly address systematic risk but also to support its proper functioning (i.e financial stability).Such design requires: 1) Well managed financial institutions with effective corporate governance and risk management system 2) Disclosure requirements sufficient to support market discipline. 3)Proper mechanisms for resolving problem institution and 4) Mechanisms to protect financial services consumers in the event of financial institutions failure.

Keywords: FIIs, BSE, sensex, global impact

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Authors: Ehsan Khorshidian, Afshin Farahbakhsh, Sina Aghili

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Enzymes are promising biocatalysts for many organic reactions. They have excellent features like high activity, specificity and selectivity, and can catalyze under mild and environment friendly conditions. Epoxy-activated supports are almost-ideal ones to perform very easy immobilization of proteins and enzymes at both laboratory and industrial scale. The activated epoxy supports (chitosan/alginate, Eupergit C) may be very suitable to achieve the multipoint covalent attachment of proteins and enzymes, therefore, to stabilize their three-dimensional structure. The enzyme is firstly covalently immobilized under conditions pH 7.0 and 10.0. The remaining groups of the support are blocked to stop additional interaction between the enzyme and support by mercaptoethanol or Triton X-100. The results show support allowed obtaining biocatalysts with high immobilized protein amount and hydrolytic activity. The immobilization of lipases on epoxy support may be considered as attractive tool for obtaining highly active biocatalysts to be used in both aqueous and anhydrous aqueous media.

Keywords: immobilization of enzymes, epoxy supports, enzyme multipoint covalent attachment, microbial lipases

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Authors: Daniela Istrati, Camelia Vizireanu, Camelia Grozavu, Rodica Mihaela Dinica

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In last years, eating habits have changed, and snacking has become more common. Snacking habits, including eating whole fruit, vegetables and crackers, were found to contribute to better overall diet quality, while consuming snacks such as cookies, pastries, sweets, milk desserts and soft drinks was associated with poorer diet quality. The nutritional quality of the snack is very important and choosing nutritious foods as snacks can be beneficial for our health. For this reason, the development of functional snacks bars represents a necessity for this niche market. The aim of this work was to develop some formulations of energizing snack bars with high dietary fibers and antioxidant activity. Snack bars contain both fruits with antioxidant activity and components (cereals and seeds) rich in carbohydrates and polyunsaturated fats that provide energy during sports activities, physical and mental stress. Three types of samples were prepared and stored in refrigerated conditions at 40°C for 30 days. The first sample (S1) contains wheat germs, raw pumpkin seeds, toasted oat flakes, flaxseeds flour, cinnamon honey, raw sunflower seeds, sea buckthorn, amaranth flour, cinnamon and olive oil. The second sample (S2) has the same composition as the first, less flour and cinnamon flour and the honey used was ginger, honey. The third sample (S3) is like the first less amaranth flour and the honey used was buckthorn sea honey. The physicochemical, antioxidant activity, polyphenolic and flavonoid content and sensorial characteristics of the samples were investigated. Results showed that snacks bars had important level of extracted phenolics, flavonoids, fibers, proteins, carbohydrates and fats. Therefore, snack bars may be a convenient functional food, offering an important source of flavonoids and polyphenols, a healthy alternative to a poor diet quality, with balanced nutritional and sensory characteristics that recommend it in the diet of all consumers concerned with maintaining health. Acknowledgment: This study has been founded by the Francophone University Agency, Project Réseau régional dans le domaine de la santé, la nutrition et la sécurité alimentaire (SaIN), No. at Dunarea de Jos University of Galati 21899/ 06.09.2017

Keywords: antioxidant activity, functional food, sea buckthorn, snack bars

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Authors: Vagolu S. Krishna, Shan Zheng, Estharla M. Rekha, Luke W. Guddat, Dharmarajan Sriram

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Tuberculosis (TB) remains a major threat to human health. This due to the fact that current drug treatments are less than optimal as well as the rising occurrence of multi drug-resistant and extensively drug-resistant strains of the etiological agent, Mycobacterium tuberculosis (Mt). Given the wide-spread significance of this disease, we have undertaken a design and evaluation program to discover new anti-TB drug leads. Here, our attention is focused on ketol-acid reductoisomerase (KARI), the second enzyme in the branched-chain amino acid biosynthesis pathway. Importantly, this enzyme is present in bacteria but not in humans, making it an attractive proposition for drug discovery. In the present work, we used high-throughput virtual screening to identify seventeen potential inhibitors of KARI using the Birla Institute of Technology and Science in-house database. Compounds were selected based on high docking scores, which were assigned as the result of favourable interactions between the compound and the active site of KARI. The Ki values for two leads, compounds 14 and 16 are 3.71 and 3.06 µM, respectively for Mt KARI. To assess the mode of binding, 100 ns molecular dynamics simulations for these two compounds in association with Mt KARI were performed and showed that the complex was stable with an average RMSD of less than 2.5 Å for all atoms. Compound 16 showed an MIC of 2.06 ± 0.91 µM and a 1.9 fold logarithmic reduction in the growth of Mt in an infected macrophage model. The two compounds exhibited low toxicity against murine macrophage RAW 264.7 cell lines. Thus, both compounds are promising candidates for development as an anti-TB drug leads.

Keywords: ketol-acid reductoisomerase, macrophage, molecular docking and dynamics, tuberculosis

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Authors: Leelavinothan Pari , Ayyasamy Rathinam

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Diabetes mellitus (DM) is a major and growing public health problem throughout the world. Pterocarpus marsupium (Roxb.) (Family: Fabaceae) is widely used as a traditional medicine to treat various diseases including diabetes. However, the molecular mechanism of Pterocarpus marsupium has not been investigated so far. Two fractions (2.5% and 5%) of extract from the medicinal plant, Pterocarpus marsupium (PME) were conducted in a dose dependent manner in streptozotocin (45 mg/kg b.w.) induced type 2 diabetic rats. Each fraction of PME was administered to diabetic rats intragastrically at a dose of 50, 100 and 200 mg/kg b.w for 45 days. The effective dose 200 mg/kg b.w of 5% fraction was more pronounced in reducing the levels of blood glucose (95.65 mg/dL) and glycosylated hemoglobin (HbA1c) (0.41 mg/g Hb), and increasing the plasma insulin (16.20 µU/mL) level. Moreover, PME (200 mg/kg b.w) significantly ameliorated lipid peroxidation products (thiobarbituric reactive substances, lipid hydroperoxides) enzymatic (superoxide dismutase, catalase and glutathione peroxidase) and non-enzymatic antioxidants (Vitamin C, Vitamin E and reduced glutathione) levels. The altered activities of the key enzymes of lipid metabolism along with the lipid profile in diabetic rats were significantly reverted to near normal levels by the administration of PME 5% 200 mg/kg b.w fraction. PME (200 mg/kg b.w) has the ability to reduce the inflammatory cytokines, such as TNF-α, IL-6 mRNA, as well as protein expression and apoptotic marker, such as caspase-3 enzyme in diabetic hepatic tissue. The above biochemical findings were also supported by histological studies such as improvement in pancreas and liver. Pterocarpus marsupium could effectively reduce the hyperglycemia, oxidative-stress, inflammation and hyperlipedimea in diabetic rats; hence it could be a useful drug in the management of diabetes without any side effects.

Keywords: diabetes mellitus, streptozotocin, Pterocarpus marsupium, lipid peroxidation, Antioxidants, inflammatory cytokines

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Authors: Yuyun, Fritz Akhmad Nuzir, Bart Julien Dewancker

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Check-in locations on social media provide information about an individual’s location. The millions of units of data generated from these sites provide knowledge for human activity. In this research, we used a geolocation service and users’ texts posted on Twitter social media to analyze human mobility. Our research will answer the questions; what are the movement patterns of a citizen? And, how far do people travel in the city? We explore the people trajectory of 201,118 check-ins and 22,318 users over a period of one month in Makassar city, Indonesia. To accommodate individual mobility, the authors only analyze the users with check-in activity greater than 30 times. We used sampling method with a systematic sampling approach to assign the research sample. The study found that the individual movement shows a high degree of regularity and intensity in certain places. The other finding found that the average distance an urban inhabitant can travel per day is as far as 9.6 km.

Keywords: mobility, check-in, distance, Twitter

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Authors: Rituparna Nath, Shawn J. Marshall

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Glaciers are one of the main sensitive climatic indicators, as they respond strongly to small climatic shifts. We develop a flow line model of glacier dynamics to simulate the past and future extent of glaciers in the Canadian Rocky Mountains, with the aim of coupling this model within larger scale regional climate models of glacier response to climate change. This paper will focus on glacier-climate modeling and reconstructions of glacier volume from the Little Ice Age (LIA) to present for Athabasca Glacier, Alberta, Canada. Glacier thickness, volume and mass change will be constructed using flow line modelling and examination of different climate scenarios that are able to give good reconstructions of LIA ice extent. With the availability of SPOT 5 imagery, Digital elevation models and GIS Arc Hydro tool, ice catchment properties-glacier width and LIA moraines have been extracted using automated procedures. Simulation of glacier mass change will inform estimates of meltwater run off over the historical period and model calibration from the LIA reconstruction will aid in future projections of the effects of climate change on glacier recession. Furthermore, the model developed will be effective for further future studies with ensembles of glaciers.

Keywords: flow line modeling, Athabasca Glacier, glacier mass balance, Remote Sensing, Arc hydro tool, little ice age

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Authors: Marcela Karmazínová, Michal Štrba, Miln Pilgr

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The paper deals with the problems of the actual behavior, failure mechanism and load-carrying capacity of the special bolt connection developed and intended for the assembly connections of truss main girders of perspective railway temporary steel bridges. Within the framework of this problem solution, several types of structural details of assembly joints have been considered as the conceptual structural design. Based on the preliminary evaluation of advantages or disadvantages of these ones, in principle two basic structural configurations so-called “tooth” and “splice-plate” connections have been selected for the subsequent detailed investigation. This investigation is mainly based on the experimental verification of the actual behavior, strain and failure mechanism and corresponding strength of the connection, and on its numerical modeling using FEM. This paper is focused only on the cyclic loading (fatigue) tests results of “splice-plate” connections and their evaluation, which have already been finished. Simultaneously with the fatigue tests, the static loading tests have been realized too, but these ones, as well as FEM numerical modeling, are not the subject of this paper.

Keywords: Bolt assembly connection, cyclic loading, failure mechanisms, fatigue strength, steel structure, structural detail category, temporary railway bridge

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Authors: Juan C. Martínez-Alfaro, Aracely Zúñiga, Fernando Ruíz-Zarate

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In recent years, the Katahdin sheep breeds have been one of the breeds with greater acceptance by sheep farmers in southwestern Mexico. The Hair Sheep breeds from tropical latitudes (16° to 21° North Latitude) show low estrus activity from January to May. By contrast, these breeds of sheep exhibit high estrus activity from August to December. However, the reproductive management of Hair Sheep crossbred is very limited, independently of the socioeconomic levels of sheep farmers. Thus, in crossbred of Hair Sheep, occurrence of lambing is greater in autumn (84%) than spring (16%). In this sense, the aim of this study was to determine the lambing in Crossbred of Katahdin sheep during different seasons of the year. The Hypothesis was that in crossbred of Katahdin sheep, the lambing period has a behavior seasonal in the Southwestern Mexico. The study design consisted in evaluating the lambing proportion in one herds of Katahdin ewes crossbred during one year (October 1st, 2015 to October 1st, 2016). The study was realized in a farm located in the municipality of Jiquipilas, in the State of Chiapas, Mexico (16° North Latitude). A total of 40 female sheep homogeneous in terms of physical condition, age and physiological state were selected; and they were fed in grazing continuous, mainly with Africa star grass (Cynodon lemfuensis) and they are provided with water and mineral salts ad libitum; during the dry season, the ewes were supplemented with a diet of maize and sorghum, and the reproductive management was continuous mating. The lambing proportion was analyzed by chi-squared test, using SAS statistical software. The proportion of Katahdin ewes crossbred that lambed during the study period was high (100%; 40/40), the prolificacy was 1.42 (lamb/lambing). The proportion of lambing was higher (P<0.05) in autumn (67.5%; 27/40), than winter, spring and summer (32.5%; 13/40; 0%; 0/40; 0%; 0/40; respectively). The proportion of lambing was greater (P<0.05) in November (50%; 20/40), compared to October, December and January (2.5%; 1/40; 27.5%; 11/40; 20%; 8/40, respectively). The results are consistent with the fact that in the Hair Sheep Breeds, the lambing appears behave seasonally. The most important finding is that the lambing period in the crossbred of Katahdin Sheep is similar to the crossbred of Hair Sheep in tropical regions of Mexico. Therefore, the period of greater sexual activity occurs in the spring season. In conclusion, the period of lambing in crossbred of Katahdin ewes appears behave seasonally. Further researches to assess the ovarian activity in different breeds of Hair Ewes are under assessment.

Keywords: Katahdin ewes, lambing, prolificacy, seasonality

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Authors: Haileyesus Tessema Alemneh, Abiyu Enyew Molla, Oluwole Daniel Makinde

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Introduction: Faba bean is one of the most important grown plants worldwide for humans and animals. Several biotic and abiotic elements have limited the output of faba beans, irrespective of their diverse significance. Many faba bean pathogens have been reported so far, of which the most important yield-limiting disease is chocolate spot disease (Botrytis fabae). The dynamics of disease transmission and decision-making processes for intervention programs for disease control are now better understood through the use of mathematical modeling. Currently, a lot of mathematical modeling researchers are interested in plant disease modeling. Objective: In this paper, a deterministic mathematical model for chocolate spot disease (CSD) on faba bean plant with an optimal control model was developed and analyzed to examine the best strategy for controlling CSD. Methodology: Three control interventions, quarantine (u2), chemical control (u3), and prevention (u1), are employed that would establish the optimal control model. The optimality system, characterization of controls, the adjoint variables, and the Hamiltonian are all generated employing Pontryagin’s maximum principle. A cost-effective approach is chosen from a set of possible integrated strategies using the incremental cost-effectiveness ratio (ICER). The forward-backward sweep iterative approach is used to run numerical simulations. Results: The Hamiltonian, the optimality system, the characterization of the controls, and the adjoint variables were established. The numerical results demonstrate that each integrated strategy can reduce the diseases within the specified period. However, due to limited resources, an integrated strategy of prevention and uprooting was found to be the best cost-effective strategy to combat CSD. Conclusion: Therefore, attention should be given to the integrated cost-effective and environmentally eco-friendly strategy by stakeholders and policymakers to control CSD and disseminate the integrated intervention to the farmers in order to fight the spread of CSD in the Faba bean population and produce the expected yield from the field.

Keywords: CSD, optimal control theory, Pontryagin’s maximum principle, numerical simulation, cost-effectiveness analysis

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Authors: Oluseun A. Akinsorotan, Louise K. Gentle, Md. Mofakkarul Islam, Richard W. Yarnell

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High levels of anthropogenic activity such as habitat destruction, poaching and encroachment into natural habitat have resulted in significant global wildlife declines. In order to protect wildlife, many protected areas such as national parks have been created. However, it is argued that many protected areas are only protected in name and are often exposed to continued, and often illegal, anthropogenic pressure. In West African protected areas, declines of large mammals have been documented between 1962 and 2008. This study aimed to produce occupancy estimates of the remaining large mammal fauna in the third largest National Park in Nigeria, Old Oyo, and to compare the estimates with historic estimates while also attempting to quantify levels of illegal anthropogenic activity using a multi-disciplinary approach. Large mammal populations and levels of illegal anthropogenic activity were assessed using empirical field data (camera trapping and transect surveys) in combination with data from questionnaires completed by local villagers and park rangers. Four of the historically recorded species in the park, lion (Panthera leo), hunting dog (Lycaon pictus), elephant (Loxodonta africana) and buffalo (Syncerus caffer) were not detected during field studies nor were they reported by respondents. In addition, occupancy estimates of hunters and illegal grazers were higher than the majority of large mammal species inside the park. This finding was reinforced by responses from the villagers and rangers who’s perception was that large mammal densities in the park were declining, and that a large proportion of the local people were entering the park to hunt wild animals and graze their domestic livestock. Our findings also suggest that widespread poverty and a lack of alternative livelihood opportunities, culture of consuming bushmeat, lack of education and awareness of the value of protected areas, and weak law enforcement are some of the reasons for the illegal activity. Law enforcement authorities were often constrained by insufficient on-site personnel and a lack of modern equipment and infrastructure to deter illegal activities. We conclude that there is a need to address the issue of illegal hunting and livestock grazing, via provision of alternative livelihoods, in combination with community outreach programmes that aim to improve conservation education and awareness and develop the capacity of the conservation authorities in order to achieve conservation goals. Our findings have implications for the conservation management of all protected areas that are available for exploitation by local communities.

Keywords: camera trapping, conservation, extirpation, illegal grazing, large mammals, national park, occupancy estimates, poaching

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