Search results for: drug loading

Authors: Xianjia Meng, Chuanyong Qu

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Compact bone produces fatigue damage under the inevitable physiological load. The accumulation of fatigue damage can change the bone’s micro-structure at different scales and cause the catastrophic failure eventually. However, most tests were limited to the macroscopic modulus of bone and there is a need to assess the microscopic modulus during fatigue progress. In this paper, nano-identation was used to investigate the bone specimen subjected to four point bending. The microscopic modulus of the same area were measured at different degrees of damage including fracture. So microscopic damage can be divided into three stages: first, the modulus decreased rapidly and then They fell slowly, before fracture the decline became fast again. After fracture, the average modulus decreased by 20%. The results of inner and outer planes explained the influence of compressive and tensile loads on modulus. Both the compressive and tensile moduli decreased with the accumulation of damage. They reached the minimum at ending and increased after fracture. The modulus evolution under different strains were revealed by the side. They all fell slowly and then fast with the accumulation of damage. The fractured results indicated that the elastic modulus decreased obviously at the high strain while decreased less at the low strain. During the fatigue progress, there was a significant difference in modulus at low degree of damage. However, the dispersed modulus tended to be similar at high degree of damage, but they became different again after the failure.

Keywords: fatigue damage, fracture, microscopic modulus, bone, nano-identation

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Authors: Gómez Romero Jacob, García Peña Elvia Inés

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The co-digestion process of crude cheese whey (CCW) with fruit vegetable waste (FVW) for biohydrogen production was investigated in batch and continuous systems, in stirred 1.8 L bioreactors at 37°C. Five different C/N ratios (7, 17, 21, 31, and 46) were tested in batch systems. While, in continuous system eight conditions were evaluated, hydraulic retention time (from 60 to 10 h) and organic load rate (from 21.96 to 155.87 g COD/L d). Data in batch tests showed a maximum specific biohydrogen production rate of 10.68 mmol H2/Lh and a biohydrogen yield of 449.84 mL H2/g COD at a C/N ratio of 21. In continuous co-digestion system, the optimum hydraulic retention time and organic loading rate were 17.5 h and 80.02 g COD/L d, respectively. Under these conditions, the highest volumetric production hydrogen rate (VPHR) and hydrogen yield were 11.02 mmol H2/L h, 800 mL H2/COD, respectively. A pyrosequencing analysis showed that the main acclimated microbial communities for co-digestion studies consisted of Bifidobacterium, with 85.4% of predominance. Hydrogen producing bacteria such as Klebsiella (9.1%), Lactobacillus (0.97%), Citrobacter (0.21%), Enterobacter (0.27%), and Clostridium (0.18%) were less abundant at this culture period. The microbial population structure was correlated with the lactate, acetate, and butyrate profiles obtained. Results demonstrated that the co-digestion of CCW with FVW improves biohydrogen production due to a better nutrient balance and improvement of the system’s buffering capacity.

Keywords: acclimatation, biohydrogen, co-digestion, microbial community

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Authors: Naser Alenezi, Ibrahim Alsakkaf, Osama Eid

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The main objective of this study is to develop an independent reliability based code for reinforced concrete (R/C) structural components and elements solely for the State of Kuwait and its neighboring countries. The proposed code will take into account the harsh Kuwait’s harsh environment, loading conditions and material strengths. The method for developing such a code is based on structural reliability theory that takes into accounts the specific geographical and the various prescribed societal environment of the Kuwait region. These methods were developed according to the following four components: (1) loads, (2) structural strength, (3) reliability analysis, and (4) achieving target reliability levels (reliability index ’s ). The final product from this study will be a design code for R/C structural elements that include beams and columns, and some other structural members. This reliability-based LRFD design code will provide appropriate, easy, fast, and economical approach for designing R/C structural elements such as, beams and columns, for both houses and bridges, and other concrete structures. In addition, this reliability-based codified design of R/C beams, columns, and, possibly, concrete slabs will improve the design and serviceability of R/C bridge and building systems in Kuwait and neighboring GCC countries. Also, it has the potential to reduce the cost of new concrete structures, as fewer materials are used with more design efficiency.

Keywords: live laod, design, evaluation, structural building

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Authors: Shahnaz Mansouri, David Martin, Xiao Dong Chen, Meng Wai Woo

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Ultrafine hydrophobic and non-water-soluble drugs can increase the percentage of absorbed compared to their initial dosage. This paper provides a scalable new method of making ultrafine particles of substantially insoluble water compounds specifically, submicron particles of ethanol soluble and water insoluble pharmaceutical materials by steaming an ethanol droplet to prepare a suspension and then followed by immediate drying. This suspension is formed by adding evaporated water molecules as an anti-solvent to the solute of the samples and in early stage of precipitation continued to dry by evaporating both solvent and anti-solvent. This fine particle formation has produced fast dispersion powder in water. The new method is an extension of the antisolvent vapour precipitation technique which exposes a droplet to an antisolvent vapour with reference to the dissolved materials within the droplet. Ultrafine vitamin D3 and ibuprofen particles in the submicron ranges were produced. This work will form the basis for using spray dryers as high-throughput scalable micro-precipitators.

Keywords: single droplet drying, nano size particles, non-water-soluble drugs, precipitators

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Authors: Mohammad Reza Baradaran, Farhad Hamzezarghani, Mehdi Rastegari Ghiri, Zahra Mirsanjari

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Passive control methods can be utilized to build earthquake resistant structures, and also to strengthen the vulnerable ones. One of the most effective, yet simple passive control methods is the use of vertical shear-links (VSL) in systems with eccentric bracing. In fact, vertical shear-links dissipate the earthquake energy and act like a ductile fuse. In this paper, we studied the effect of this system in increasing the ductility and energy dissipation and also modeled the behavior of this type of eccentric bracing, and compared the hysteresis diagram of the modeled samples with the laboratory samples. We studied several samples of frames with vertical shear-links in order to assess the behavior of this type of eccentric bracing. Each of these samples was modeled in finite element software ANSYS 9.0, and was analyzed under the static cyclic loading. It was found that vertical shear-links have a more stable hysteresis loops. Another analysis showed that using honeycomb beams as the horizontal beam along with steel reinforcement has no negative effect on the hysteresis behavior of the sample.

Keywords: vertical shear-link, passive control, cyclic analysis, energy dissipation, honeycomb beam

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Authors: Sam Weber, Deepak Mishra, Susan Wilde, Elizabeth Kramer

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The frequency and severity of cyanobacteria harmful blooms (CyanoHABs) have been increasing over time, with point and non-point source eutrophication and shifting climate paradigms being blamed as the primary culprits. Excessive nutrients, warm temperatures, quiescent water, and heavy and less regular rainfall create more conducive environments for CyanoHABs. CyanoHABs have the potential to produce a spectrum of toxins that cause gastrointestinal stress, organ failure, and even death in humans and animals. To promote enhanced, proactive CyanoHAB management, risk modeling using geospatial tools can act as predictive mechanisms to supplement current CyanoHAB monitoring, management and mitigation efforts. The risk maps would empower water managers to focus their efforts on high risk water bodies in an attempt to prevent CyanoHABs before they occur, and/or more diligently observe those waterbodies. For this research, exploratory spatial data analysis techniques were used to identify the strongest predicators for CyanoHAB blooms based on remote sensing-derived cyanobacteria cell density values for 771 waterbodies in the Georgia Piedmont and landscape characteristics of their watersheds. In-situ datasets for cyanobacteria cell density, nutrients, temperature, and rainfall patterns are not widely available, so free gridded geospatial datasets were used as proxy variables for assessing CyanoHAB risk. For example, the percent of a watershed that is agriculture was used as a proxy for nutrient loading, and the summer precipitation within a watershed was used as a proxy for water quiescence. Cyanobacteria cell density values were calculated using atmospherically corrected images from the European Space Agency’s Sentinel-2A satellite and multispectral instrument sensor at a 10-meter ground resolution. Seventeen explanatory variables were calculated for each watershed utilizing the multi-petabyte geospatial catalogs available within the Google Earth Engine cloud computing interface. The seventeen variables were then used in a multiple linear regression model, and the strongest predictors of cyanobacteria cell density were selected for the final regression model. The seventeen explanatory variables included land cover composition, winter and summer temperature and precipitation data, topographic derivatives, vegetation index anomalies, and soil characteristics. Watershed maximum summer temperature, percent agriculture, percent forest, percent impervious, and waterbody area emerged as the strongest predictors of cyanobacteria cell density with an adjusted R-squared value of 0.31 and a p-value ~ 0. The final regression equation was used to make a normalized cyanobacteria cell density index, and a Jenks Natural Break classification was used to assign waterbodies designations of low, medium, or high risk. Of the 771 waterbodies, 24.38% were low risk, 37.35% were medium risk, and 38.26% were high risk. This study showed that there are significant relationships between free geospatial datasets representing summer maximum temperatures, nutrient loading associated with land use and land cover, and the area of a waterbody with cyanobacteria cell density. This data analytics approach to CyanoHAB risk assessment corroborated the literature-established environmental triggers for CyanoHABs, and presents a novel approach for CyanoHAB risk mapping in waterbodies across the greater southeastern United States.

Keywords: cyanobacteria, land use/land cover, remote sensing, risk mapping

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Authors: Muhammad Mustafa Jafar, Syed Ashar Mahfooz, Muhammad Ejaz Saleem, Muhammad Asif Raza, Asghar Abbas, Rao Zahid Abbas, Muhammad Kasib Khan, Hafiz Muhammad Ishaq

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The Babesia gradually attained resistance against the synthetic medicines. To overcome the drug resistance, herbal therapy has gained more attention as compared to allopathic therapy. Peganumharmala (harmal) is a plant which has shown effective results against various protozoal diseases. Therefore, the present study was planned to monitor the efficacy of Peganumharmala (aqueous extract) against Babesiosis in cattle. For this purpose, a total of forty (n=40) infected animals were randomly divided into four equal groups (A, B, C, and D). Group A was treated with aqueous extract of Peganum harmala at 7.5 mg/kg, group B at 10 mg/kg and group C at 12.5 mg/kg of body weight. Group D served as a control group (normal). It was observed that there was a stabilization in hematological parameters (white and red blood cells, hemoglobin and Packed cell volume) in infected animals treated with Peganum harmala at different doses. Results of this study hence indicated that Peganum harmala extract at 12.5mg/kg BW is more effective against Babesiosis than lower doses.

Keywords: Babesiosis, cattle, control, Peganum harmala

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Authors: M. Safiqul Islam, Md Arafat Hossain Sarkar

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Brachytherapy is one of the most important cancer treatment management systems in radiotherapy department. Brachytherapy treatment is moved into High Dose Rate (HDR) after loader from Low Dose Rate (LDR) after loader due to radiation protection advantage. HDR Brachytherapy is a highly multipurpose system for enhancing cure and achieving palliation in many common cancers disease of developing countries. High-dose rate (HDR) Brachytherapy is a type of internal radiation therapy that delivers radiation from implants placed close to or inside, the tumor(s) in the body. This procedure is very effective at providing localized radiation to the tumor site while minimizing the patient’s whole body dose. Brachytherapy has proven to be a highly successful treatment for cancers of the prostate, cervix, endometrium, breast, skin, bronchus, esophagus, and head and neck, as well as soft tissue sarcomas and several other types of cancer. For the time being in our country we have 10 new HDR Remote after loading Brachytherapy. Right now 4 HDR Brachytherapy is already installed and running for patient’s treatment out of 10 HDR Brachytherapy. Ir-192 source is more comfortable than Co-60. In that case people or expert personnel prefer Ir-192 source for different kind of cancer patients. Ir-192 are economically, more flexible and familiar in our country.

Keywords: Ir-192, brachytherapy, cancer treatment, prostate, cervix, endometrium, breast, skin, bronchus, esophagus, soft tissue sarcomas

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Authors: Moses Basitere, Marshal Sherene Sheldon, Seteno Karabo Obed Ntwampe, Debbie Dejager

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In South Africa, Poultry slaughterhouses consume largest amount of freshwater and discharges high strength wastewater, which can be treated successfully at low cost using anaerobic digesters. In this study, the performance of bench-scale mesophilic Static Granular Bed Reactor (SGBR) containing fully anaerobic granules coupled with ultra-filtration (UF) membrane as a post-treatment for poultry slaughterhouse wastewater was investigated. The poultry slaughterhouse was characterized by chemical oxygen demand (COD) range between 2000 and 6000 mg/l, average biological oxygen demand (BOD) of 2375 mg/l and average fats, oil and grease (FOG) of 554 mg/l. A continuous SGBR anaerobic reactor was operated for 6 weeks at different hydraulic retention time (HRT) and an Organic loading rate. The results showed an average COD removal was greater than 90% for both the SGBR anaerobic digester and ultrafiltration membrane. The total suspended solids and fats oil and grease (FOG) removal was greater than 95%. The SGBR reactor coupled with UF membrane showed a greater potential to treat poultry slaughterhouse wastewater.

Keywords: chemical oxygen demand, poultry slaughterhouse wastewater, static granular bed reactor, ultrafiltration, wastewater

Procedia PDF Downloads 387

Authors: V. Antevska, B. Dejanova, L. Todorovska, J. Pluncevic, E. Sivevska, S. Petrovska, S. Mancevska, I. Karagjozova

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Introduction: The aim of this study was to optimise the laboratory oxidative stress (OS) markers in soccer players. Material and methods: In a number of 37 soccer players (21±3 years old) and 25 control subjects (sedenters), plasma samples were taken for d-ROMs (reactive oxygen metabolites) and NO (nitric oxide) determination. The d-ROMs test was performed by measurement of hydroperoxide levels (Diacron, Italy). For NO determination the method of nitrate enzyme reduction with the Greiss reagent was used (OXIS, USA). The parameters were taken after the training of the soccer players and were compared with the control group. Training was considered as maximal exercise treadmill test. The criteria of maximum loading for each subject was established as >95% maximal heart rate. Results: The level of d-ROMs was found to be increased in the soccer players vs. control group but no significant difference was noticed. After the training d-ROMs in soccer players showed increased value of 299±44 UCarr (p<0.05). NO showed increased level in all soccer players vs. controls but significant difference was found after the training 102±29 μmol (p<0.05). Conclusion: Due to these results we may suggest that the measuring these OS markers in sport medicine may be useful for better estimation and evaluation of the training program. More oxidative stress should be used to clarify optimization of the training intensity program.

Keywords: oxidative stress markers, soccer players, training, sport

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Authors: M. R. Noor El-Din, Marwa R. Mishrif, R. E. Morsi, E. A. El-Sharaky, M. E. Haseeb, Rania T. M. Ghanem

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This paper studies the physical and rheological behaviours of water/in/diesel fuel nanoemulsions prepared by modified low energy method. Twenty of water/in/diesel fuel nanoemulsions were prepared using mixed nonionic surfactants of sorbitan monooleate and polyoxyethylene sorbitan trioleate (MTS) at Hydrophilic-Lipophilic Balance (HLB) value of 10 and a working temperature of 20°C. The influence of the prepared nanoemulsions on the physical properties such as kinematic viscosity, density, and calorific value was studied. Also, nanoemulsion systems were subjected to rheological evaluation. The effect of water loading percentage (5, 6, 7, 8, 9 and 10 wt.%) on rheology was assessed at temperatures range from 20 to 60°C with temperature interval of 10 for time lapse 0, 1, 2 and 3 months, respectively. Results show that all of the sets nanoemulsions exhibited a Newtonian flow character of low-shear viscosity in the range of 132 up to 191 1/s, and followed by a shear-thinning region with yield value (Non-Newtonian behaviour) at high shear rate for all water ratios (5 to 10 wt.%) and at all test temperatures (20 to 60°C) for time ageing up to 3 months. Also, the viscosity/temperature relationship of all nanoemulsions fitted well Arrhenius equation with high correlation coefficients that ascertain their Newtonian behavior.

Keywords: alternative fuel, nanoemulsion, surfactant, diesel fuel

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Authors: Abass Braimah, Maha Hussein Abdallah

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The global ascendancy of terrorist attacks on building infrastructure with economic and heritage significance has increased awareness of the possibility of terrorism in Canada. Many structures in Canada that are at risk of terrorist attacks include government buildings, built many years ago of historic stone masonry construction. Although many researchers are investigating ways to retrofit masonry stone buildings to mitigate the effect of blast loadings, lack of knowledge on the dynamic behavior of historic stone masonry structures under blast loads makes it difficult to ascertain the effectiveness of the retrofitting techniques. This paper presents a review of open-source literature for the experimental and numerical stone masonry structures under blast loads. This review yielded very little information of the response of the historic stone masonry structures under blast loads. Thus, a comprehensive study is needed to understand the blast load effects on historic stone masonry buildings. The out-of-plane response of historic masonry structures to blast loads is investigated by using single-degree-of-freedom analysis. This approach presents equations that can be used effectively in the analysis of historic masonry walls to out-of-plane blast loading.

Keywords: blast loads, historical buildings, masonry structure, single-degree-of-freedom analysis

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Authors: Nihal Abdel Hamid Taha

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Crack evaluation of flexure reinforced concrete (RC) member is considered an important step in the design process, since the formation of concrete cracks depends on the possibility of exposure to various conditions(pollution, humidity,..etc.). Because of the disparity between different grades of steel in the service load stresses, this affects the cracking behavior. This paper is concerned with the crack pattern and cracking load for concrete beams with T-section reinforced with two different grades of steel at the service load levels stages up to ultimate load. A practical program has been put up to investigate the difference between reinforced steel bars with yield strength 420 N/mm2 and 500 N/mm2 through six T-section reinforced beams. The beams were tested under static- monotonic two– point service loading up to ultimate failure under flexural stresses. The influence of parameters such as clear concrete cover and concrete compressive strength are considered for each of the two grades of steel used. Cracking load, spacing and width were determined. The experimental results demonstrated that increasing the concrete strength results in both of cracking and ultimate load increase, while no significant difference in yield load for the two steel grades used. It has also become obvious, that the number of cracks was more for the lower steel strength, which is followed by decrease in crack width and spacing.

Keywords: RC beams, cracking behavior, steel stress, crack width, crack spacing

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Authors: Phuriwat Laomethakorn, Siritron Samosorn, Ramida Watanapokasin

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Cancer metastasis is the major cause of cancer-related death. Therefore searching for a compound that could inhibit cancer metastasis is necessary. 13-Butoxyberberine bromide is a berberine derivative that has not been reported an anti-metastatic effect on skin cancer cells. This study aimed to investigate the anti-metastatic effect of 13-butoxyberberine bromide on skin cancer A431 cells. The effect of 13-butoxyberberine bromide on A431 cell viability was examined by MTT assay. Suppression of cell migration and invasion in A431 cells were determined by wound healing assay, transwell migration assay, and transwell invasion assay. Metastasis proteins were determined by western blotting. The results demonstrated that 13-butoxyberberine bromide decreased A431 cell viability in a dose-dependent manner. In addition, sub-toxic concentrations of 13-butoxyberberine bromide suppressed cell migration and invasion in A431 cells. In addition, 13-butoxyberberine bromide showed anti-metastatic effects by down-regulated MMP-2 and MMP-9 expression. These findings may be useful in the development of 13-butoxyberberine bromide as an anti-metastatic drug in the future.

Keywords: 13-butoxyberberine bromide, metastasis, skin cancer, MMP

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Authors: Peter Fedichev

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We studied fundamental aspects of aging to develop a mathematical model of gene regulatory network. We show that aging manifests itself as an inherent instability of gene network leading to exponential accumulation of regulatory errors with age. To validate our approach we studied age-dependent omic data such as transcriptomes, metabolomes etc. of different model organisms and humans. We build a computational platform based on our model to identify the targets and biomarkers of aging to design new drugs against aging and age-related diseases. As biomarkers of aging, we choose the rate of aging and the biological age since they completely determine the state of the organism. Since rate of aging rapidly changes in response to an external stress, this kind of biomarker can be useful as a tool for quantitative efficacy assessment of drugs, their combinations, dose optimization, chronic toxicity estimate, personalized therapies selection, clinical endpoints achievement (within clinical research), and death risk assessments. According to our model, we propose a method for targets identification for further interventions against aging and age-related diseases. Being a biotech company, we offer a complete pipeline to develop an anti-aging drug-candidate.

Keywords: aging, longevity, biomarkers, senescence

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Authors: Ali Yasin, Ali Kamran, Muhammad Safdar

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In order to reduce the hefty cost involved in terms of time and project cost, the development and application of advanced numerical tools to address the burn-back analysis problem in solid rocket motor design and development is the need of time. Several advanced numerical schemes have been developed in recent times, but their usage in the design of propellant grain of solid rocket motors is very rare. In this paper, an advanced numerical technique named the Level-Set method has been utilized for the burn-back analysis of star grain to study the effect of geometrical parameters on ballistic performance indicators such as solid loading, neutrality, and sliver percentage. In the level set technique, simple finite difference methods may fail quickly and require more sophisticated non-oscillatory schemes for feasible long-time simulation. For internal ballistic calculations, a simplified equilibrium pressure method is utilized. Preliminary results of the operative conditions, for all the combustion time, of star grain burn-back using level set techniques are compared with published results using CAD technique to test the developed numerical model.

Keywords: solid rocket motor, internal ballistic, level-set technique, star grain

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Authors: Ihsan Burak Cam, Ferhan Balci-Torun, Ayhan Topuz, Esin Ari, Ismail Gokhan Deniz, Ilker Genc

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The seeds of Vaccaria hispanica have been used in food and pharmaceutical industry. It is an important product due to its superior starch granules, triterpenic saponins, and cyclopeptides suitable for drug delivery. V. hispanica naturally grows in different climatic regions and has genotypes that differ in terms of seed content and composition. Sixty-six V. hispanica seed specimens were collected based on the representation of the distribution in all regions of Turkey and the determination of possible genotypic differences between regions. The seeds, collected from each of the 66 locations, were grown in greenhouse conditions in Akdeniz University, Antalya. Saponin and cyclopeptide contents of the V. hispanica seeds were determined after harvest. Accelerated solvent extraction (ASE) was applied for the extraction of saponins and cyclopeptides. Cyclopeptide (segetalin A) and saponin content of V. hispanica seeds were found in the range of 0.165-0.654 g/100 g and 0.15-1.14 g/100 g, respectively. The results were found to be promising for the seeds from Turkey in terms of saponin content and quality. Acknowledgment: This study was supported by the Scientific and Research Council of Turkey (TUBITAK) (project no 112 O 136).

Keywords: Vaccaria hispanica, saponin, cyclopeptid, cow cockle seeds

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Authors: Morteza Karami, Soheila Dayani

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Deep Soil Mixing (DSM) is a soil improvement technique that involves mechanically mixing the soil with a binder material to improve its strength, stiffness, and durability. This technique is typically used in geotechnical engineering applications where weak or unstable soil conditions exist, such as in building foundations, embankment support, or ground improvement projects. In this study, the settlement of the foundation on the improved soil using the wet DSM technique has been analyzed for a case study. Before DSM production, the initial soil mixture has been determined based on the laboratory tests and then, the proper mix designs have been optimized based on the pilot scale tests. The results show that the spacing and depth of the DSM columns depend on the soil properties, the intended loading conditions, and other factors such as the available space and equipment limitations. Moreover, monitoring instruments installed in the pilot area verify that the settlement of the foundation has been placed in an acceptable range to ensure that the soil mixture is providing the required strength and stiffness to support the structure or load. As an important result, if the DSM columns touch or penetrate into the stiff soil layer, the settlement of the foundation can be significantly decreased. Furthermore, the DSM columns should be allowed to cure sufficiently before placing any significant loads on the structure to prevent excessive deformation or settlement.

Keywords: deep soil mixing, soil mixture, settlement, instrumentation, curing age

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Authors: Ugur Cihat Sakarya

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This research focuses on psychedelic trance music events in Turkey in the context of altered states of consciousness (ASC). The fieldwork that was conducted from 2018 to 2019 is the main source of the research. Participant observation method was followed in 15 selected events. To direct the musical experiences of participants, performances were also presented as a Dj. Ten of these events are open-air festivals. Five of them are indoor parties. The observations made during fieldwork and suitable answers for inference from the interviews with participants, artists, DJs, and volunteers were selected, compiled, and presented. In the result, findings showed that these activities are perceived as temporary autonomous areas by the participants both in time and space and that these activities are suitable areas for expressing themselves as a group (psyfamily) against mainstream culture. It has been observed that the elements that complement the altered states of consciousness in these events are music, visual arts, drug use, and desire to experience spiritual experiences. It is thought that this first academic study -about this topic in Turkey- will open a door for future researches.

Keywords: consciousness, psychedelic, psytrance, rave, Turkey

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Authors: Watchareewan Thongsaard, Ratirat Sangpayap, Maneekarn Namsa-Aid

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Thunbergia laurifolia Linn. (TL) is a herbal medicine which has been used as an antidote for several poisonous agents including insecticides and as a component of a mixture of crude extracts to treat drug addicted patients. The aim of this study is to examine the level of dopamine in nucleus accumbens after chronic pre-administration of TL in ethanol addicted rats. Male Wistar rats weigh 200-250 g received TL methanol extract (200mg/kg, orally) 60 minutes before 20% ethanol (1 g/kg, i.p.) for 30 days. The nucleus accumbens was removed and tested for dopamine by HPLC-ECD. The level of dopamine was significantly increased by chronic ethanol administration, whereas the chronic TL extract administration did not cause a difference in dopamine level when compared to control. Moreover, the pre-treatment of TL extract before ethanol significantly reduced the dopamine level in nucleus accumbens to normal level when compared with chronic ethanol administration alone. These results suggested that the increase in dopamine level in the nucleus accumbens by chronic ethanol administration is the cause of ethanol addiction, and this effect is prevented by chronic TL pre-administration. Furthermore, chronic TL extract administration alone did not cause the changes in dopamine level in the nucleus accumbens, indicating that TL itself did not cause addiction.

Keywords: Thunbergia laurifolia Linn., alcohol addiction, dopamine, nucleus accumbens

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Authors: Sijia Hu

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Tensile creep tests were performed along the normal direction on the as-solutioned (AS) and as-aged (AA) samples of a commercial ZK60 alloy in this work. The results showed that the AA sample obtained a stronger 0.2% proof stress but a poorer creep resistance in comparison to the AS sample. It was revealed that the creep deformation in the AS sample was attributed to basal slip and twinning, while the creep behavior of the AA sample was controlled by basal slip, pyramidal slip and twinning. Besides, the reasons for the poorer creep resistance of the AA sample were unveiled. Pyramidal dislocations towards various moving directions were found to accelerate the creep deformation, and basal dislocations kinking at twin boundaries were found to induce heavy stress concentration. Furthermore, massive dynamic precipitates, including beta 1 prime and beta 2 prime types, were formed in the AS sample during the creep exposure, contributing to the superior creep resistance. But in the AA sample, plentiful beta 1 prime and beta 2 prime phases generated during the prior peak-aging treatment dissolved into the matrix fast and only beta 1 prime re-precipitated during the creep process. With the decreased area fractions of precipitates, the age-hardening effect slacked off and failed to enhance the creep resistance.

Keywords: Mg alloy, creep, precipitation, microstructure

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Authors: Afaf Bouchoucha, Karima Si Larbi, Mohamed Amine Bourouaia, Salah.Boulanouar, Safia.Djabbar

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The synthesis, characterization and comparative biological study of manganese (II) and copper (II) complexes with an heterocyclic ligand used in pharmaceutical field (Scheme 1), were reported. Two kinds of complexes were obtained with derivative sulfonamide, [M (L)₂ (H₂O)₂].H₂O and [M (L)₂ (Cl)₂]3H₂O. These complexes have been prepared and characterized by elemental analysis, FAB mass, ESR magnetic measurements, FTIR, UV-Visible spectra and conductivity. Their stability constants have been determined by potentiometric methods in a water-ethanol (90:10 v/v) mixture at a 0.2 mol l-1 ionic strength (NaCl) and at 25.0 ± 0.1 ºC using Sirko program. DFT calculations were done using B3LYP/6-31G(d) and B3LYP/LanL2DZ. The antimicrobial activity of ligand and complexes against the species Escherichia coli, P. aeruginosa, Klebsiella pneumoniae, S. aureus, Bacillus subtilisan, Candida albicans, Candida tropicalis, Saccharomyces, Aspergillus fumigatus and Aspergillus terreus has been carried out and compared using agar-diffusion method. Also, the toxicity study was evaluated on synchesis complexes using Mice of NMRI strain.

Keywords: hetterocyclic ligand, complex, stability constant, antimicrobial activity, DFT, acute and genotoxicity study

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Authors: K. Żak, S. Przetocka, R. Kitel, K. Guzik, B. Musielak, S. Malicki, G. Dubin, T. A. Holak

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Studies on tumor genesis revealed a number of factors that may potentially serve as molecular targets for immunotherapies. One of such promising targets are PD1 and PDL1 proteins. PD1 (Programmed cell death protein 1) is expressed by activated T cells and plays a critical role in modulation of the host's immune response. One of the PD1 ligands -PDL1- is expressed by macrophages, monocytes and cancer cells which exploit it to avoid immune attack. The notion of the mechanisms used by cancer cells to block the immune system response was utilized in the development of therapies blocking PD1-PDL1 interaction. Up to date, human PD1-PDL1 complex has not been crystallized and structure of the mouse-human complex does not provide a complete view of the molecular basis of PD1-PDL1 interactions. The purpose of this study is to obtain crystal structure of the human PD1-PDL1 complex which shall allow rational design of small molecule inhibitors of the interaction. In addition, the study presents results of binding small-molecules to PD1 and fragment docking towards PD1 protein which will facilitate the design and development of small–molecule inhibitors of PD1-PDL1 interaction.

Keywords: PD1, PDL1, cancer, small molecule, drug discovery

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Authors: Jeonghun Lee

Abstract:

In this study, we investigated the relationship between stress and thyroid dysfunction in such patients who underwent thyroidectomy. This study included 101 patients who underwent thyroidectomy from January 2015 to June 2020 and experienced hypothyroidism. The included patients had good drug compliance with the same dosage of levothyroxine (LT4). The male-to-female ratio was 1:4.6, and the mean age was 45.4 years at surgery and 50.2 years at stressful events. Eighteen patients underwent lobectomies and, of these, 12 did not take LT4. The mean follow-up period was 49(8-93) months. Statistical analyses were performed using the paired t-test, Wilcoxon signed-rank test, and McNemer test using PROC MIXED with SAS 9.4. Forty-five patients (44.6%) had hypothyroidism with thyroid-stimulating hormone (TSH) >10 μIU/mL. There was distress in 81 patients and eustress in 10 patients. TSH levels increased during a mean 5.8 months (min 1, max 12) in 24 patients who specified the date of their life events. Even though each patient took the same dose of LT4, when the patients were under stress, both the free T4 and T3 decreased and TSH increased, regardless of whether the patient experienced distress or eustress (P <0.001). While adjusting for the effect of the free T4 and T3, TSH increased significantly in the patients after stress (P <0.001). For patients with thyroid cancer who are simultaneously experiencing life events, TSH may be used as a stress biomarker to enable the implementation of appropriate treatment and counseling strategies.

Keywords: endocrine, thyroid, thyroid function, biomarker, stress

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Authors: Shao-Hsuan Chien, Ju-Hui Fu

Abstract:

Parkinson’s disease (PD) is a degenerative disorder of the central nervous system that is characterized by progressive loss of dopaminergic neurons in the substantia nigra pars compacta and motor impairment. Aggregation of α-synuclein in neuronal cells plays a key role in this disease. At present, therapeutics for PD provides moderate symptomatic benefit but is not able to delay the development of this disease. Current efforts for the treatment of PD are to identify new drugs that show slow or arrest progressive course of PD by interfering with a disease-specific pathogenetic process in PD patients. Maackiain is a bioactive compound isolated from the roots of the Chinese herb Sophora flavescens. The purpose of the present study was to assess the potential for maackiain to ameliorate PD in Caenorhabditis elegans models. Our data reveal that maackiain prevents α-synuclein accumulation in the transgenic Caenorhabditis elegans model and also improves dopaminergic neuron degeneration, food-sensing behavior, and life-span in 6-hydroxydopamine-induced Caenorhabditis elegans model, thus indicating its potential as a candidate antiparkinsonian drug.

Keywords: maackiain, Parkinson’s disease, dopaminergic neurons, α-Synuclein

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Authors: Flavia Laffleur, Andreas Bernkop-Schnürch

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Purpose: This study was aimed to investigate preactivated thiomers for their mucoadhesive potential. Methods: Accordingly, chitosan-thioglycolic-mercaptonicotinamide conjugates (chitosan-TGA-MNA) were synthesized by the oxidative S-S coupling of chitosan-thioglycolic acid (chitosan-TGA) with 6-mercaptonicotin amide (MNA). Unmodified chitosan, chitosan-TGA (thiomers) and chitosan-TGA-MNA conjugates were compressed into test discs to investigate cohesive properties, cytotoxicity assays and mucoadhesion studies. Results: Due to the immobilization of MNA, the chitosan-TGA-MNA conjugates exhibit comparatively higher swelling properties and cohesive properties corresponding unmodified chitosan. On the rotating cylinder, discs based on chitosan-TGA-MNA conjugates displayed 3.1-fold improved mucoadhesion time compared to thiolated polymers. Tensile study results were found in good agreement with rotating cylinder results. Moreover, preactivated thiomers showed higher stability. All polymers were found non-toxic over Caco-2 cells. Conclusion: On the basis of achieved results the pre activated thiomeric therapeutic agent seems to represent a promising generation of mucoadhesive polymers which are safe to use for a prolonged residence time to target the mucosa.

Keywords: biomedical application, drug delivery, polymer, thiomer

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Authors: Q. J. Yang

Abstract:

This paper presents a case study of geotechnical design of bridge foundations and approaches in hilly granite formation in northern New South Wales of Australia. Firstly, the geological formation and existing cut slope conditions which have high risks of rock fall will be described. The bridge has three spans to be constructed using balanced cantilever method with a middle span of 150 m. After concept design option engineering, it was decided to change from pile foundation to pad footing with ground anchor system to optimize the bridge foundation design. The geotechnical design parameters were derived after two staged site investigations. The foundation design was carried out to satisfy both serviceability limit state and ultimate limit state during construction and in operation. It was found that the pad footing design was governed by serviceability limit state design loading cases. The design of bridge foundation also considered presence of weak rock layer intrusion and a layer of “no core” to ensure foundation stability. The precast mass concrete block system was considered for the retaining walls for the bridge approaches to resolve the constructability issue over hilly terrain. The design considered the retaining wall block sliding stability, while the overturning and internal stabilities are satisfied.

Keywords: pad footing, Hilly formation, stability, block works

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Authors: Rorlinda Yusof, Siti Aishah Hassan, Afifah Mohamad Radzi, Mohd Hakimie Zainal Abidin, Amran Rasli, Inderbir Sandhu

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The purpose of this study is to examine the self-identities of gifted and talented students and the relationship between self-identity and academic accomplishment. A random sample of 300 students enrolled in a secondary education programme at the Pusat GENIUS@pintar Negara was chosen as respondents of a 151-item holistic-identity component development tool. The validity of the instrument was assessed using Principal Components Analysis and Factor Analysis via an inter-Item Correlation Matrix (Loading values 0.44 to 0.86), which resulted in the formation of eight dimensions. The Cronbach's Alpha was calculated to determine the instrument's reliability (the overall result was 0.98). The results showed that students' holistic-identity profiles were relatively high (mean=4.09, standard deviation=0.449). In addition, spiritual identity received the greatest mean score (4.34) out of the eight components of identity investigated, while leadership identity received the lowest mean score (3.88). A conceptual framework for Islamic school leadership is recommended to implement spiritual values without differentiation to harmonize spiritual and intellectual intelligence among all the students. Some benchmarking studies with other centres for gifted and talented students are recommended for further research.

Keywords: holistic self-identity, academic achievement, self-development programme, counselling services, gifted and talented students

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Authors: U. L. Fulco, E. L. Albuquerque, José X. Lima Neto, L. R. Da Silva

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The binding of the nonsteroidal anti-inflammatory drug ibuprofen (IBU) to human serum albumin (HSA) is investigated using density functional theory (DFT) calculations within a fragmentation strategy. Crystallographic data for the IBU–HSA supramolecular complex shows that the ligand is confined to a large cavity at the subdomain IIIA and at the interface between the subdomains IIA and IIB, whose binding sites are FA3/FA4 and FA6, respectively. The interaction energy between the IBU molecule and each amino acid residue of these HSA binding pockets was calculated using the Molecular Fractionation with Conjugate Caps (MFCC) approach employing a dispersion corrected exchange–correlation functional. Our investigation shows that the total interaction energy of IBU bound to HSA at binding sites of the fatty acids FA3/FA4 (FA6) converges only for a pocket radius of at least 8.5 °A, mainly due to the action of residues Arg410, Lys414 and Ser489 (Lys351, Ser480 and Leu481) and residues in nonhydrophobic domains, namely Ile388, Phe395, Phe403, Leu407, Leu430, Val433, and Leu453 (Phe206, Ala210, Ala213, and Leu327), which is unusual. Our simulations are valuable for a better understanding of the binding mechanism of IBU to albumin and can lead to the rational design and the development of novel IBU-derived drugs with improved potency.

Keywords: ibuprofen, human serum albumin, density functional theory, binding energies

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Authors: M. A. Ahmed, N. Basha, I. V. Nsahlai

Abstract:

This study determined the effectiveness of selected anthementics (Ivermectin 1% (IVM), Closantel 7.5% (CST) and a combination Abamectin 0.08% and Praziquantel 1.5% (CAP) currently being used in SA. Gender, initial egg per gram (EPG) and initial live weight aided in blocking animals into groups, each group was randomly treated with one of four drug treatments comprising: the untreated control (D0), IVM, CST, and CAP. Animals grazed throughout on infested pasture. Rectal faeces were collected on days 0, 7, 14, and 21 for determining EPG. Faeces were mixed per group and incubated to identify and determine the abundance of larval forms of Haemonchus, Trichostrongylus, Strongyloides, Namatodirus, and Cooperia species. Differences between treatments changed over time. On day7 IVM, CST, and CAP depressed EPG to 0.66, 0.37 and 0.80 of their respective starting values whilst EPG increased 1.39 times for D0. Thereafter, EPG increased consistently for all drugs; CST recorded the lowest values. Haemonchus, Trichostrongylus, Strongyloides, Namatodirus and Coperia species contributed respectively 60%, 30%, 6%, 3%, and 1% of the larval forms on day 0; and 78%, 8%, 11%, 1%, 2% on day 21. Larval forms increased for Haemonchus species but decreased for Trichostrongylus species over time. Closantel was the most effective dewormer. Haemonchus Spp. were least affected whilst Trichostrongylus Spp. were the most affect by all drugs.

Keywords: anthementics, faecal egg count, L3 larvae, sheep

Procedia PDF Downloads 508