Search results for: multiple drug resistance
Commenced in January 2007
Frequency: Monthly
Edition: International
Paper Count: 9201

Search results for: multiple drug resistance

6861 Development and Characterization of a Fluorinated-Ethylene-Propylene (FEP) Polymer Coating on Brass Faucets

Authors: S. Zouari, H. Ghorbel, H. Liao, R. Elleuch

Abstract:

Research is increasingly moving towards the use of surface treatment processes to limit environmental effects. Electrolytic plating has traditionally been seen as a way to protect brass products, especially faucets, from mechanical and chemical damage. However, this method was not effective industrially, economically and ecologically. The aim of this work is to develop non-usual polymer coatings for brass faucets in order to improve the performance of brass and to replace electrolytic chromium coatings, thereby reducing environmental impact. Fluorinated-Ethylene-Propylene polymer (FEP) was chosen for its excellent mechanical and chemical properties and its good environmental performance. This coating was developed by spraying (painting) process onto brass substrates. The coatings obtained were characterized using a scanning electron microscope to evaluate the morphology of the deposits and their porosity rate. Grid adhesion, surface energy and corrosion tests (salt spray) were also performed to evaluate the mechanical and chemical behavior of these coatings properly. The results show that the deposits obtained have a homogeneous microstructure with a very low porosity rate. The results of the grid adhesion test prove the conformity of the test according to the NF077 standard. The coatings have a hydrophobic character following the low values of surface energy obtained and a very good resistance to corrosion. These results are interesting and may represent real technological issues in the industrial field.

Keywords: FEP coatings, spraying process, brass, adhesion, surface energy, corrosion resistance

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6860 Predictor Factors in Predictive Model of Soccer Talent Identification among Male Players Aged 14 to 17 Years

Authors: Muhamad Hafiz Ismail, Ahmad H., Nelfianty M. R.

Abstract:

The longitudinal study is conducted to identify predictive factors of soccer talent among male players aged 14 to 17 years. Convenience sampling involving elite respondents (n=20) and sub-elite respondents (n=20) male soccer players. Descriptive statistics were reported as frequencies and percentages. The inferential statistical analysis is used to report the status of reliability, independent samples t-test, paired samples t-test, and multiple regression analysis. Generally, there are differences in mean of height, muscular strength, muscular endurance, cardiovascular endurance, task orientation, cognitive anxiety, self-confidence, juggling skills, short pass skills, long pass skills, dribbling skills, and shooting skills for 20 elite players and sub-elite players. Accordingly, there was a significant difference between pre and post-test for thirteen variables of height, weight, fat percentage, muscle strength, muscle endurance, cardiovascular endurance, flexibility, BMI, task orientation, juggling skills, short pass skills, a long pass skills, and dribbling skills. Based on the first predictive factors (physical), second predictive factors (fitness), third predictive factors (psychological), and fourth predictive factors (skills in playing football) pledged to the soccer talent; four multiple regression models were produced. The first predictive factor (physical) contributed 53.5 percent, supported by height and percentage of fat in soccer talents. The second predictive factor (fitness) contributed 63.2 percent and the third predictive factors (psychology) contributed 66.4 percent of soccer talent. The fourth predictive factors (skills) contributed 59.0 percent of soccer talent. The four multiple regression models could be used as a guide for talent scouting for soccer players of the future.

Keywords: soccer talent identification, fitness and physical test, soccer skills test, psychological test

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6859 Optimal Design Solution in "The Small Module" Within the Possibilities of Ecology, Environmental Science/Engineering, and Economics

Authors: Hassan Wajid

Abstract:

We will commend accommodating an environmentally friendly architectural proposal that is extremely common/usual but whose features will make it a sustainable space. In this experiment, the natural and artificial built space is being proposed in such a way that deals with Environmental, Ecological, and Economic Criteria under different climatic conditions. Moreover, the criteria against ecology-environment-economics reflect in the different modules which are being experimented with and analyzed by multiple research groups. The ecological, environmental, and economic services are provided used as units of production side by side, resulting in local job creation and saving resources, for instance, conservation of rainwater, soil formation or protection, less energy consumption to achieve Net Zero, and a stable climate as a whole. The synthesized results from the collected data suggest several aspects to consider when designing buildings for beginning the design process under the supervision of instructors/directors who are responsible for developing curricula and sustainable goals. Hence, the results of the research and the suggestions will benefit the sustainable design through multiple results, heat analysis of different small modules, and comparisons. As a result, it is depleted as the resources are either consumed or the pollution contaminates the resources.

Keywords: optimization, ecology, environment, sustainable solution

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6858 Optimization of Heat Insulation Structure and Heat Flux Calculation Method of Slug Calorimeter

Authors: Zhu Xinxin, Wang Hui, Yang Kai

Abstract:

Heat flux is one of the most important test parameters in the ground thermal protection test. Slug calorimeter is selected as the main sensor measuring heat flux in arc wind tunnel test due to the convenience and low cost. However, because of excessive lateral heat transfer and the disadvantage of the calculation method, the heat flux measurement error of the slug calorimeter is large. In order to enhance measurement accuracy, the heat insulation structure and heat flux calculation method of slug calorimeter were improved. The heat transfer model of the slug calorimeter was built according to the energy conservation principle. Based on the heat transfer model, the insulating sleeve of the hollow structure was designed, which helped to greatly decrease lateral heat transfer. And the slug with insulating sleeve of hollow structure was encapsulated using a package shell. The improved insulation structure reduced heat loss and ensured that the heat transfer characteristics were almost the same when calibrated and tested. The heat flux calibration test was carried out in arc lamp system for heat flux sensor calibration, and the results show that test accuracy and precision of slug calorimeter are improved greatly. In the meantime, the simulation model of the slug calorimeter was built. The heat flux values in different temperature rise time periods were calculated by the simulation model. The results show that extracting the data of the temperature rise rate as soon as possible can result in a smaller heat flux calculation error. Then the different thermal contact resistance affecting calculation error was analyzed by the simulation model. The contact resistance between the slug and the insulating sleeve was identified as the main influencing factor. The direct comparison calibration correction method was proposed based on only heat flux calibration. The numerical calculation correction method was proposed based on the heat flux calibration and simulation model of slug calorimeter after the simulation model was solved by solving the contact resistance between the slug and the insulating sleeve. The simulation and test results show that two methods can greatly reduce the heat flux measurement error. Finally, the improved slug calorimeter was tested in the arc wind tunnel. And test results show that the repeatability accuracy of improved slug calorimeter is less than 3%. The deviation of measurement value from different slug calorimeters is less than 3% in the same fluid field. The deviation of measurement value between slug calorimeter and Gordon Gage is less than 4% in the same fluid field.

Keywords: correction method, heat flux calculation, heat insulation structure, heat transfer model, slug calorimeter

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6857 The Effects of the “War on Drugs” on Black and Latino Youth

Authors: Aniya Everette

Abstract:

In June of 1971, President Richard Nixon made his first public declaration regarding the “War on Drugs,” deeming it America’s number one public enemy. Since then, the drug war has been a divisive topic in the US. Black and brown children have been unfairly targeted and imprisoned at alarming rates as a result of this policy, which has had a negative effect on them. Black and Latino youth have faced significant obstacles that have impacted their educational opportunities, employment prospects, and general quality of life due to harsh mandatory sentences, aggressive policing tactics, and racial profiling.

Keywords: war, drugs, crime, racial profiling

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6856 Synergistic Effect of Eugenol Acetate with Betalactam Antibiotic on Betalactamase and Its Bioinformatics Analysis

Authors: Vinod Nair, C. Sadasivan

Abstract:

Beta-lactam antibiotics are the most frequently prescribed medications in modern medicine. The antibiotic resistance by the production of enzyme beta-lactamase is an important mechanism seen in microorganisms. Resistance to beta-lactams mediated by beta-lactamases can be overcome successfully with the use of beta-lactamase inhibitors. New generations of the antibiotics contain mostly synthetic compounds, and many side effects have been reported for them. Combinations of beta-lactam and beta-lactamase inhibitors have become one of the most successful antimicrobial strategies in the current scenario of bacterial infections. Plant-based drugs are very cheap and having lesser adverse effect than synthetic compounds. The synergistic effect of eugenol acetate with beta-lactams restores the activity of beta-lactams, allowing their continued clinical use. It is reported here the enhanced inhibitory effect of phytochemical, eugenol acetate, isolated from the plant Syzygium aromaticum with beta-lactams on beta-lactamase. The compound was found to have synergistic effect with the antibiotic amoxicillin against antibiotic-resistant strain of S.aureus. The enzyme was purified from the organism and incubated with the compound. The assay showed that the compound could inhibit the enzymatic activity of beta-lactamase. Modeling and molecular docking studies indicated that the compound can fit into the active site of beta-lactamase and can mask the important residue for hydrolysis of beta-lactams. The synergistic effects of eugenol acetate with beta-lactam antibiotics may justify, the use of these plant compounds for the preparation of β-lactamase inhibitors against β-lactam resistant S.aureus.

Keywords: betalactamase, eugenol acetate, synergistic effect, molecular modeling

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6855 Porul: Option Generation and Selection and Scoring Algorithms for a Tamil Flash Card Game

Authors: Anitha Narasimhan, Aarthy Anandan, Madhan Karky, C. N. Subalalitha

Abstract:

Games can be the excellent tools for teaching a language. There are few e-learning games in Indian languages like word scrabble, cross word, quiz games etc., which were developed mainly for educational purposes. This paper proposes a Tamil word game called, “Porul”, which focuses on education as well as on players’ thinking and decision-making skills. Porul is a multiple choice based quiz game, in which the players attempt to answer questions correctly from the given multiple options that are generated using a unique algorithm called the Option Selection algorithm which explores the semantics of the question in various dimensions namely, synonym, rhyme and Universal Networking Language semantic category. This kind of semantic exploration of the question not only increases the complexity of the game but also makes it more interesting. The paper also proposes a Scoring Algorithm which allots a score based on the popularity score of the question word. The proposed game has been tested using 20,000 Tamil words.

Keywords: Porul game, Tamil word game, option selection, flash card, scoring, algorithm

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6854 Prevalence and Drug Susceptibility Profiles of Bacterial Urinary Tract Infections Isolated among Diabetes Mellitus Patients at Bosaso Health Centers

Authors: Said Abdirasak Abidrahman, Ibrahim Mohamed

Abstract:

Background: Urinary Tract Infections (UTIs) are the commonest infections described among diabetes mellitus patients. More often, empirical antimicrobial therapy is initiated before the laboratory results are made available with minimal treatment success. The knowledge of the etiology and antibiotic susceptibility patterns of the organisms causing urinary tract infections among diabetes mellitus patients remains scarce, despite its vitality. This study sought to determine the prevalence, bacteria species, and drug susceptibility patterns of common causes of urinary tract infections among diabetes mellitus patients attending Bosaso health centers. Materials and methods: We conducted a cross-sectional study involving adult diabetic patients at Bosaso health centers between the months of May and July 2020. Laboratory assay of mid-stream urine samples was done to isolate bacteria causes of UTIs. These were biochemically identified using Gram stain, Kligler iron agar (KIA), Indole test, citrate, urea, coagulase, catalase, motility agar, and lysine iron agar. Their antibiotic susceptibility pattern for the isolated organisms was made for Ampicillin 10μg, Ciprofloxacin 5μg, Cotrimoxazole 25μg, Gentamycin 10μg, Ceftriaxone 10μg, and determined using the Kirby Bauer Disc Diffusion method. Results: Of 177 participants, 69 (39.0%) were males and 108 (61.0%) were females. Their mean age was 33.1 years (range; 18-67 years). Of these, 14.7% (26/177) of the samples revealed significant growth (>= 105 CFU/mL) giving a prevalence of 14.9 % (95% CI: 10.6 to 16.3). The organisms isolated were Escherichia coli -50% (N=13), Klebsiella pneumonia 30.8% (N=8), Staphylococcus aureus 15.4% (N=4), and unidentified organism 3.8% (N=1), and these were associated with such socio-demographic factors like history of catheterization and sexual activity. Antibiotic susceptibility to the commonly used agents for treating UTIs indicated higher sensitivity to Gentamicin and Ceftriaxone.

Keywords: antimicrobials, bacteria, urinary tract infections, diabetes

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6853 Familial Exome Sequencing to Decipher the Complex Genetic Basis of Holoprosencephaly

Authors: Artem Kim, Clara Savary, Christele Dubourg, Wilfrid Carre, Houda Hamdi-Roze, Valerie Dupé, Sylvie Odent, Marie De Tayrac, Veronique David

Abstract:

Holoprosencephaly (HPE) is a rare congenital brain malformation resulting from the incomplete separation of the two cerebral hemispheres. It is characterized by a wide phenotypic spectrum and a high degree of locus heterogeneity. Genetic defects in 16 genes have already been implicated in HPE, but account for only 30% of cases, suggesting that a large part of genetic factors remains to be discovered. HPE has been recently redefined as a complex multigenic disorder, requiring the joint effect of multiple mutational events in genes belonging to one or several developmental pathways. The onset of HPE may result from accumulation of the effects of multiple rare variants in functionally-related genes, each conferring a moderate increase in the risk of HPE onset. In order to decipher the genetic basis of HPE, unconventional patterns of inheritance involving multiple genetic factors need to be considered. The primary objective of this study was to uncover possible disease causing combinations of multiple rare variants underlying HPE by performing trio-based Whole Exome Sequencing (WES) of familial cases where no molecular diagnosis could be established. 39 families were selected with no fully-penetrant causal mutation in known HPE gene, no chromosomic aberrations/copy number variants and without any implication of environmental factors. As the main challenge was to identify disease-related variants among a large number of nonpathogenic polymorphisms detected by WES classical scheme, a novel variant prioritization approach was established. It combined WES filtering with complementary gene-level approaches: transcriptome-driven (RNA-Seq data) and clinically-driven (public clinical data) strategies. Briefly, a filtering approach was performed to select variants compatible with disease segregation, population frequency and pathogenicity prediction to identify an exhaustive list of rare deleterious variants. The exome search space was then reduced by restricting the analysis to candidate genes identified by either transcriptome-driven strategy (genes sharing highly similar expression patterns with known HPE genes during cerebral development) or clinically-driven strategy (genes associated to phenotypes of interest overlapping with HPE). Deeper analyses of candidate variants were then performed on a family-by-family basis. These included the exploration of clinical information, expression studies, variant characteristics, recurrence of mutated genes and available biological knowledge. A novel bioinformatics pipeline was designed. Applied to the 39 families, this final integrated workflow identified an average of 11 candidate variants per family. Most of candidate variants were inherited from asymptomatic parents suggesting a multigenic inheritance pattern requiring the association of multiple mutational events. The manual analysis highlighted 5 new strong HPE candidate genes showing recurrences in distinct families. Functional validations of these genes are foreseen.

Keywords: complex genetic disorder, holoprosencephaly, multiple rare variants, whole exome sequencing

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6852 Relationship between Hepatokines and Insulin Resistance in Childhood Obesity

Authors: Mustafa Metin Donma, Orkide Donma

Abstract:

Childhood obesity is an important clinical problem because it may lead to chronic diseases during the adulthood period of the individual. Obesity is a metabolic disease associated with low-grade inflammation. The liver occurs at the center of metabolic pathways. Adropin, fibroblast growth factor-21 (FGF-21), and fetuin-A are hepatokines. Due to the immense participation of the liver in glucose metabolism, these liver-derived factors may be associated with insulin resistance (IR), which is a phenomenon discussed within the scope of obesity problems. The aim of this study is to determine the concentrations of adropin, FGF-21, and fetuin-A in childhood obesity, to point out possible differences between the obesity groups, and to investigate possible associations among these three hepatokines in obese and morbidly obese children. A total of one hundred and thirty-two children were included in the study. Two obese groups were constituted. The groups were matched in terms of mean ± SD values of ages. Body mass index values of obese and morbidly obese groups were 25.0 ± 3.5 kg/m² and 29.8 ± 5.7 kg/m², respectively. Anthropometric measurements including waist circumference, hip circumference, head circumference, and neck circumference were recorded. Informed consent forms were taken from the parents of the participants. The ethics committee of the institution approved the study protocol. Blood samples were obtained after overnight fasting. Routine biochemical tests, including glucose- and lipid-related parameters, were performed. Concentrations of the hepatokines (adropin, FGF-21, fetuin A) were determined by enzyme-linked immunosorbent assay. Insulin resistance indices such as homeostasis model assessment for IR (HOMA-IR), alanine transaminase-to aspartate transaminase ratio (ALT/AST), diagnostic obesity notation model assessment laboratory index, diagnostic obesity notation model assessment metabolic syndrome index as well as obesity indices such as diagnostic obesity notation model assessment-II index, and fat mass index were calculated using the previously derived formulas. Statistical evaluation of the study data as well as findings of the study was performed by SPSS for Windows. Statistical difference was accepted significant when p is smaller than 0.05. Statistically significant differences were found for insulin, triglyceride, high-density lipoprotein cholesterol levels of the groups. A significant increase was observed for FGF-21 concentrations in the morbidly obese group. Higher adropin and fetuin-A concentrations were observed in the same group in comparison with the values detected in the obese group (p > 0.05). There was no statistically significant difference between the ALT/AST values of the groups. In all of the remaining IR and obesity indices, significantly increased values were calculated for morbidly obese children. Significant correlations were detected between HOMA-IR and each of the hepatokines. The highest one was the association with fetuin-A (r=0.373, p=0.001). In conclusion, increased levels observed in adropin, FGF-21, and fetuin-A have shown that these hepatokines possess increasing potential going from obese to morbid obese state. Out of the correlations found with the IR index, the most affected hepatokine was fetuin-A, the parameter possibly used as the indicator of the advanced obesity stage.

Keywords: adropin, fetuin A, fibroblast growth factor-21, insulin resistance, pediatric obesity

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6851 Vitamin D Status in Tunisian Obese Patients

Authors: O. Berriche, R. Ben Othmen, H. Sfar, H. Abdesslam, S. Bou Meftah, S. Bhouri, F. Mahjoub, C. Amrouche, H. Jamoussi

Abstract:

Introduction: Although current evidence emphasizes a high prevalence of vitamin D deficiency and an inverse association between serum 25-hydroxyvitamin D (25-OHD) concentration and obesity, no studies have been conducted in Tunisian obese. The objectives of our study were to estimate the vitamin D deficiency in obese, identify risk factors for vitamin D deficiency, demonstrating a possible association between vitamin D levels and metabolic parameters. Methods: This was a descriptive study of 100 obese 18-65 year-old. Anthropometric measurements were determined. Fasting blood samples were assessed for the following essays : serum calcium, 25 OH vitamin D, inorganic phosphorus, fasting glucose, HDL, LDL cholesterol and triglyceride. Insulin resistance was evaluated by fasting insulin, HOMA-IR and HOMA-ß. Consumption of foods riche in vitamin D, sunscreen use, wearing protective clothes and exposed surface were assessed through applied questionnaires. Results: The deficit of vitamin D (< 30 ng/ml) among obese was 98,8%. Half of them had a rate < 10ng/ml. Environmental factors involved in vitamin D deficiency are : the veil (p = 0,001), wearing protective clothes (p = 0,04) and the exposed surface (p = 0,011) and dietary factors are represented by the daily caloric intake (p = 0,0001). The percent of fat mass was negatively related to vitamin D levels (p = 0,01) but not with BMI (p = 0,11) or waist circumference (p = 0,88). Similarly, lipid and glucose profile had no link with vitamin D. We found no relationship between Insulin resistance and vitamin D levels. Conclusion: At the end of our study, we have identified a very important vitamin D deficiency among obese. Dosage and systematic supplementation should be applied and for that physician awareness is needed.

Keywords: insulinresistance, risk factors, obesity, vitamin D

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6850 A Study on Pattern of Acute Poisoning in Patients Admitted to Emergency Wards in a Tertiary Care Hospital

Authors: Sathvika Reddy, Devi Revathi

Abstract:

Background: In India, deliberate self-harm (DSH) with poisoning agents carries a significant impact on morbidity and mortality. Changes in the patterns of poisoning vary across various geographical locations. It is important to know the patterns in a given region in order to facilitate rapid clinical diagnosis, appropriate treatment to reduce associated morbidity and mortality. Aim and Objective: To study the patterns, treatment outcomes of acute poisoning in patients admitted to emergency wards in a tertiary care hospital and to provide poison information services. Materials and Methods: This study was conducted at M.S Ramaiah Memorial and Teaching Hospital from November 2016 to March 2017. The patient’s data was obtained from patient case sheet, interaction with health care professionals, interviewing patients and their caretakers (if possible), and were documented in a suitably designed form. Results: The study involved 131 patients with a mean age of 27.76 ± 15.5 years. Majority of the patients were in the age group 21-30 years, literates (n=53) dwelling in urban (n=113) areas belonging to upper middle class (n=50). Analgesics and antipyretics were commonly utilized in intentional drug overdosage (n=49). Envenomation constituted n=21(16.03%). Furthermore, a significant relationship was observed between marital status and self-poisoning (n=64) (P < 0.001) which commonly occurred through oral ingestion. The outcomes were correlated with the GCS and PSS system and n=85 recovered, n=17 were discharged against medical advice, and n=4 died, and n=4 were lost to follow up respectively. The poison information queries include drug overdose (n=29) and management related queries (n=22) provided majorly by residents (n=45) to update knowledge (n=11) and for better patient care (n=40). Conclusion: The trend in poisoning is dynamic. Medications were identified as the main cause of poisoning in urban areas of India. Educational programs with more emphasis on preventive measures are necessary to create awareness among the general public.

Keywords: poisoning, suicides, clinical pharmacist, envenomation, poison information services

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6849 Constructing a Bayesian Network for Solar Energy in Egypt Using Life Cycle Analysis and Machine Learning Algorithms

Authors: Rawaa H. El-Bidweihy, Hisham M. Abdelsalam, Ihab A. El-Khodary

Abstract:

In an era where machines run and shape our world, the need for a stable, non-ending source of energy emerges. In this study, the focus was on the solar energy in Egypt as a renewable source, the most important factors that could affect the solar energy’s market share throughout its life cycle production were analyzed and filtered, the relationships between them were derived before structuring a Bayesian network. Also, forecasted models were built for multiple factors to predict the states in Egypt by 2035, based on historical data and patterns, to be used as the nodes’ states in the network. 37 factors were found to might have an impact on the use of solar energy and then were deducted to 12 factors that were chosen to be the most effective to the solar energy’s life cycle in Egypt, based on surveying experts and data analysis, some of the factors were found to be recurring in multiple stages. The presented Bayesian network could be used later for scenario and decision analysis of using solar energy in Egypt, as a stable renewable source for generating any type of energy needed.

Keywords: ARIMA, auto correlation, Bayesian network, forecasting models, life cycle, partial correlation, renewable energy, SARIMA, solar energy

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6848 An Investigation into the Crystallization Tendency/Kinetics of Amorphous Active Pharmaceutical Ingredients: A Case Study with Dipyridamole and Cinnarizine

Authors: Shrawan Baghel, Helen Cathcart, Biall J. O'Reilly

Abstract:

Amorphous drug formulations have great potential to enhance solubility and thus bioavailability of BCS class II drugs. However, the higher free energy and molecular mobility of the amorphous form lowers the activation energy barrier for crystallization and thermodynamically drives it towards the crystalline state which makes them unstable. Accurate determination of the crystallization tendency/kinetics is the key to the successful design and development of such systems. In this study, dipyridamole (DPM) and cinnarizine (CNZ) has been selected as model compounds. Thermodynamic fragility (m_T) is measured from the heat capacity change at the glass transition temperature (Tg) whereas dynamic fragility (m_D) is evaluated using methods based on extrapolation of configurational entropy to zero 〖(m〗_(D_CE )), and heating rate dependence of Tg 〖(m〗_(D_Tg)). The mean relaxation time of amorphous drugs was calculated from Vogel-Tammann-Fulcher (VTF) equation. Furthermore, the correlation between fragility and glass forming ability (GFA) of model drugs has been established and the relevance of these parameters to crystallization of amorphous drugs is also assessed. Moreover, the crystallization kinetics of model drugs under isothermal conditions has been studied using Johnson-Mehl-Avrami (JMA) approach to determine the Avrami constant ‘n’ which provides an insight into the mechanism of crystallization. To further probe into the crystallization mechanism, the non-isothermal crystallization kinetics of model systems was also analysed by statistically fitting the crystallization data to 15 different kinetic models and the relevance of model-free kinetic approach has been established. In addition, the crystallization mechanism for DPM and CNZ at each extent of transformation has been predicted. The calculated fragility, glass forming ability (GFA) and crystallization kinetics is found to be in good correlation with the stability prediction of amorphous solid dispersions. Thus, this research work involves a multidisciplinary approach to establish fragility, GFA and crystallization kinetics as stability predictors for amorphous drug formulations.

Keywords: amorphous, fragility, glass forming ability, molecular mobility, mean relaxation time, crystallization kinetics, stability

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6847 Evaluation of Antimicrobial Activity of Different Dithiolethiones

Authors: Zehour Rahmani, Messouda Dekmouche, Mohamed Hadjadj, Mokhtar Saidi

Abstract:

In the last decades of the nineteenth century, the study of disease – causing microorganisms became concentrated on bacteria and largely institutionalized. In earlier years, the scientists interested in bacteria had originally been chemists like Pasteur, physicists like Tyndall, or botanists like Cohn and ward. For this reason, the objective of this research was to evaluate the potential of some dithiolethiones on standard microorganism strains as well as multi-drug resistant bacteria, which were isolated from hospitals. Recent studies have demonstrated, that several dithiolethione compounds, particularly (3H-1,2-dithiole-3-thione), exhibit the biological activities against several bacteria.

Keywords: bacteria, dithiolethiones, microorganism, potential

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6846 Design, Synthesis and in-vitro Antitumor Evaluation of Some Novel Substituted Quinazoline Derivatives

Authors: Adel S. El-Azab, Alaa A. M. Abdel-Aziz, Ibrahim A. Al-Suwaidan, Amer M. Alanazi

Abstract:

A novel series of 2,3,6-trisubstitute quinazolinone were designed, synthesized, and evaluated for their in-vitro antitumor activity. 3 (Benzylideneamino)-6-chloro-2-p-tolylquinazolin-4(3H)-One, 2-[(4-oxo-3-phenethyl-3,4-dihydroquinazolin-2-yl)thio]-N-(3,4;5-trimethoxyphenyl) acetamide and 3-(3-benzyl-6-methyl-4-oxo-3, 4-dihydroquinazolin-2-ylthio)-N-(3,4,5-trimethoxyphenyl) propanamide have shown amazing broad spectrum antitumor activity with mean GI50; 15.8, 3.16, and 7.4 μM respectively compared to known Quinazoline Derivatives antitumor drug 5-FU mean GI50=22.6 μM.

Keywords: quinazoline derivatives, in vitro antitumor, synthesis, 5-FU, NCI

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6845 Enhanced High-Temperature Strength of HfNbTaTiZrV Refractory High-Entropy Alloy via Al₂O₃ Reinforcement

Authors: Bingjie Wang, Qianqian Qang, Nan Lu, Xiubing Liang, Baolong Shen

Abstract:

Novel composites of HfNbTaTiZrV refractory high-entropy alloy (RHEA) reinforced with 0-5 vol.% Al₂O₃ particles have been synthesized by vacuum arc melting. The microstructure evolution, compressive mechanical properties at room and elevated temperatures, as well as strengthening mechanism of the composites, are analyzed. The HfNbTaTiZrV RHEA reinforced with 4 vol.% Al₂O₃ displays excellent phase stability at elevated temperatures. A superior compressive yield strength of 2700 MPa at room temperature, 1392 MPa at 800 °C, and 693 MPa at 1000 °C has been obtained for this composite. The improved yield strength results from multiple strengthening mechanisms caused by Al₂O₃ addition, including interstitial strengthening, grain boundary strengthening, and dispersion strengthening. Besides, the effects of interstitial strengthening increase with the temperature and is the main strengthening mechanism at elevated temperatures. These findings not only promote the development of oxide-reinforced RHEAs for challenging engineering applications but also provide guidelines for the design of light refractory materials with multiple strengthening mechanisms.

Keywords: Al₂O₃-reinforcement, HfNbTaTiZrV, refractory high-entropy alloy, interstitial strengthening

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6844 Stakeholders Perspectives on the Social Determinants of Health and Quality of Life in Aseer Healthy Cities

Authors: Metrek Almetrek, Naser Alqahtani, Eisa Ghazwani, Mona Asiri, Mohammed Alqahtani, Magboolah Balobaid

Abstract:

Background: Advocacy of potential for community coalitions to positively address social determinants of health and quality of life, little is known about the views of stakeholders involved in such efforts. This study sought to assess the provinces leaders’ perspectives about social determinants related to the Health Neighborhood Initiative (HNI), a new county effort to support community coalitions. Method and Subjects: We used a descriptive, qualitative study using personal interviews in 2022. We conducted it in the community coalition's “main cities committees” set across service planning areas that serve vulnerable groups located in the seven registered healthy cities to WHO (Abha, Tareeb, Muhayel, Balqarn, Alharajah, Alamwah, and Bisha). We conducted key informant interviews with 76 governmental, profit, non-profit, and community leaders to understand their perspectives about the HNI. As part of a larger project, this study focused on leaders’ views about social determinants of health related to the HNI. All interviews were audio-recorded and transcribed. An inductive approach to coding was used, with text segments grouped by social determinant categories. Results: Provinces leaders described multiple social determinants of health and quality of life that were relevant to the HNI community coalitions: housing and safety, community violence, economic stability, city services coordination and employment and education. Leaders discussed how social determinants were interconnected with each other and the need for efforts to address multiple social determinants simultaneously to effectively improve health and quality of life. Conclusions: Community coalitions have an opportunity to address multiple social determinants of health and quality of life to meet the social needs of vulnerable groups. Future research should examine how community coalitions, like those in the HNI, can actively engage with community members to identify needs and then deliver evidence-based care.

Keywords: social determinants, health and quality of life, vulnerable groups, qualitative research

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6843 Machine Learning Approach for Mutation Testing

Authors: Michael Stewart

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Mutation testing is a type of software testing proposed in the 1970s where program statements are deliberately changed to introduce simple errors so that test cases can be validated to determine if they can detect the errors. Test cases are executed against the mutant code to determine if one fails, detects the error and ensures the program is correct. One major issue with this type of testing was it became intensive computationally to generate and test all possible mutations for complex programs. This paper used reinforcement learning and parallel processing within the context of mutation testing for the selection of mutation operators and test cases that reduced the computational cost of testing and improved test suite effectiveness. Experiments were conducted using sample programs to determine how well the reinforcement learning-based algorithm performed with one live mutation, multiple live mutations and no live mutations. The experiments, measured by mutation score, were used to update the algorithm and improved accuracy for predictions. The performance was then evaluated on multiple processor computers. With reinforcement learning, the mutation operators utilized were reduced by 50 – 100%.

Keywords: automated-testing, machine learning, mutation testing, parallel processing, reinforcement learning, software engineering, software testing

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6842 Determining the Efficacy of Phenol, Sodium Hypochlorite and Ethanol for Inactivation of Carbapenem-Resistant Strain of Acinetobacter baumannii

Authors: Deepika Biswas

Abstract:

Acinetobacter baumannii, a hospital-acquired pathogen, causes nosocomial infections including pneumonia, urinary tract infection, and secondary meningitis. Carbapenem is most effective antibiotics against it. Its increased resistance to carbapenems has been a rising global concern. Antibiotics such as carbapenem are unable to use on hospital setups to eradicate A. baumannii, hence different concentrations of disinfectants including phenol; sodium hypochlorite and ethanol are increasingly being used. The objective of the present study is to find an effective concentration of above disinfectants against carbapenem-resistant strain RS307 of A. baumannii. Growth kinetics of RS307 has been determined using UV-Vis spectrophotometer in the presence and absence of disinfectants in triplicate and its standard deviation has also been calculated which make the results more reliable. Differential growth curves were plotted, which showed the effective concentration among all the concentrations of phenol, sodium hypochlorite and ethanol. On disc diffusion assay, antimicrobial effect was observed by comparing all the concentrations of disinfectants to check its synergy with imipenem, most effective carbapenem. All the results collectively revealed that 0.5% phenol, 0.5% sodium hypochlorite, and 70% ethanol could preferably be used as disinfectant for hospital setup against the carbapenem-resistant strain of A. baumannii. SDS PAGE analysis showed differential expression in the protein profile of A. baumannii after treatment. The present study highlighted that few disinfectants even in low concentration had shown better antimicrobial activity hence may be recommended for regular use in the hospitals, which will be cost effective and less harmful.

Keywords: Acenatobacter bomunii, phenol, sodium hypoclirite, ethanol, carbapenem resistance, disinfectant

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6841 Knowledge, Attitude and Beliefs Towards Polypharmacy Amongst Older People Attending Family Medicine Clinic at the Aga Khan University Hospital, Nairobi, Kenya (AKUHN) Sub-Saharan Africa-Qualitative Study

Authors: Maureen Kamau, Gulnaz Mohamoud, Adelaide Lusambili, Njeri Nyanja

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Life expectancy has increased over the last century amongst older individuals, and in particular, those 60 years and over. The World Health Organization estimates that the world's population of persons over 60 years will rise to 22 per cent by the year 2050. Ageing is associated with increasing disability, multiple chronic conditions, and an increase in the use of health services. These multiple chronic conditions are managed with polypharmacy. Polypharmacy has numerous adverse effects including non-adherence, poor compliance to the various medications, reduced appetite, and risk of fall. Studies on polypharmacy and ageing are few and poorly understood especially in low and middle - income countries. The aim of this study was to explore the knowledge, attitudes and beliefs of older people towards polypharmacy. A qualitative study of 15 patients aged 60 years and above, taking more than five medications per day were conducted at the Aga Khan University using Semi-structured in-depth interviews. Three interviews were pilot interviews, and data analysis was performed on 12 interviews. Data were analyzed using NVIVO 12 software. A thematic qualitative analysis was carried out guided by Braun and Clarke (2006) framework. Themes identified; - knowledge of their co-morbidities and of the medication that older persons take, sources of information about medicines, and storage of the medication, experiences and attitudes of older patients towards polypharmacy both positive and negative, older peoples beliefs and their coping mechanisms with polypharmacy. The study participants had good knowledge on their multiple co-morbidities, and on the medication they took. The patients had positive attitudes towards medication as it enhanced their health and well-being, and enabled them to perform their activities of daily living. There was a strong belief among older patients that the medications were necessary for their health. All these factors enhanced compliance to the multiple medication. However, some older patients had negative attitudes due to the pill burden, side effects of the medication, and stigma associated with being ill. Cost of healthcare was a concern, with most of the patients interviewed relying on insurance to cover the cost of their medication. Older patients had accepted that the medication they were prescribed were necessary for their health, as it enabled them to complete their activities of daily living. Some concerns about the side effects of the medication arose, and brought about the need for patient education that would ensure that the patients are aware of the medications they take, and potential side effects. The effect that the COVID 19 pandemic had in the healthcare of the older patients was evident by the number of the older patients avoided coming to the hospital during the period of the pandemic. The relationship with the primary care physician and the older patients is an important one, especially in LMICs such as Kenya, as many of the older patients trusted the doctors wholeheartedly to make the best decision about their health and about their medication. Prescription review is important to avoid the use of potentially inappropriate medication.

Keywords: polypharmacy, older patients, multiple chronic conditions, Kenya, Africa, qualitative study, indepth interviews, primary care

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6840 Preparation and in vivo Assessment of Nystatin-Loaded Solid Lipid Nanoparticles for Topical Delivery against Cutaneous Candidiasis

Authors: Rawia M. Khalil, Ahmed A. Abd El Rahman, Mahfouz A. Kassem, Mohamed S. El Ridi, Mona M. Abou Samra, Ghada E. A. Awad, Soheir S. Mansy

Abstract:

Solid lipid nanoparticles (SLNs) have gained great attention for the topical treatment of skin associated fungal infection as they facilitate the skin penetration of loaded drugs. Our work deals with the preparation of nystatin loaded solid lipid nanoparticles (NystSLNs) using the hot homogenization and ultrasonication method. The prepared NystSLNs were characterized in terms of entrapment efficiency, particle size, zeta potential, transmission electron microscopy, differential scanning calorimetry, rheological behavior and in vitro drug release. A stability study for 6 months was performed. A microbiological study was conducted in male rats infected with Candida albicans, by counting the colonies and examining the histopathological changes induced on the skin of infected rats. The results showed that SLNs dispersions are spherical in shape with particle size ranging from 83.26±11.33 to 955.04±1.09 nm. The entrapment efficiencies are ranging from 19.73±1.21 to 72.46±0.66% with zeta potential ranging from -18.9 to -38.8 mV and shear-thinning rheological Behavior. The stability studies done for 6 months showed that nystatin (Nyst) is a good candidate for topical SLN formulations. A least number of colony forming unit/ ml (cfu/ml) was recorded for the selected NystSLN compared to the drug solution and the commercial Nystatin® cream present in the market. It can be fulfilled from this work that SLNs provide a good skin targeting effect and may represent promising carrier for topical delivery of Nyst offering the sustained release and maintaining the localized effect, resulting in an effective treatment of cutaneous fungal infection.

Keywords: candida infections, hot homogenization, nystatin, solid lipid nanoparticles, stability, topical delivery

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6839 Synthesis of MIPs towards Precursors and Intermediates of Illicit Drugs and Their following Application in Sensing Unit

Authors: K. Graniczkowska, N. Beloglazova, S. De Saeger

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The threat of synthetic drugs is one of the most significant current drug problems worldwide. The use of drugs of abuse has increased dramatically during the past three decades. Among others, Amphetamine-Type Stimulants (ATS) are globally the second most widely used drugs after cannabis, exceeding the use of cocaine and heroin. ATS are potent central nervous system (CNS) stimulants, capable of inducing euphoric static similar to cocaine. Recreational use of ATS is widespread, even though warnings of irreversible damage of the CNS were reported. ATS pose a big problem and their production contributes to the pollution of the environment by discharging big volumes of liquid waste to sewage system. Therefore, there is a demand to develop robust and sensitive sensors that can detect ATS and their intermediates in environmental water samples. A rapid and simple test is required. Analysis of environmental water samples (which sometimes can be a harsh environment) using antibody-based tests cannot be applied. Therefore, molecular imprinted polymers (MIPs), which are known as synthetic antibodies, have been chosen for that approach. MIPs are characterized with a high mechanical and thermal stability, show chemical resistance in a broad pH range and various organic or aqueous solvents. These properties make them the preferred type of receptors for application in the harsh conditions imposed by environmental samples. To the best of our knowledge, there are no existing MIPs-based sensors toward amphetamine and its intermediates. Also not many commercial MIPs for this application are available. Therefore, the aim of this study was to compare different techniques to obtain MIPs with high specificity towards ATS and characterize them for following use in a sensing unit. MIPs against amphetamine and its intermediates were synthesized using a few different techniques, such as electro-, thermo- and UV-initiated polymerization. Different monomers, cross linkers and initiators, in various ratios, were tested to obtain the best sensitivity and polymers properties. Subsequently, specificity and selectivity were compared with commercially available MIPs against amphetamine. Different linkers, such as lipoic acid, 3-mercaptopioponic acid and tyramine were examined, in combination with several immobilization techniques, to select the best procedure for attaching particles on sensor surface. Performed experiments allowed choosing an optimal method for the intended sensor application. Stability of MIPs in extreme conditions, such as highly acidic or basic was determined. Obtained results led to the conclusion about MIPs based sensor applicability in sewage system testing.

Keywords: amphetamine type stimulants, environment, molecular imprinted polymers, MIPs, sensor

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6838 Channel Estimation Using Deep Learning for Reconfigurable Intelligent Surfaces-Assisted Millimeter Wave Systems

Authors: Ting Gao, Mingyue He

Abstract:

Reconfigurable intelligent surfaces (RISs) are expected to be an important part of next-generation wireless communication networks due to their potential to reduce the hardware cost and energy consumption of millimeter Wave (mmWave) massive multiple-input multiple-output (MIMO) technology. However, owing to the lack of signal processing abilities of the RIS, the perfect channel state information (CSI) in RIS-assisted communication systems is difficult to acquire. In this paper, the uplink channel estimation for mmWave systems with a hybrid active/passive RIS architecture is studied. Specifically, a deep learning-based estimation scheme is proposed to estimate the channel between the RIS and the user. In particular, the sparse structure of the mmWave channel is exploited to formulate the channel estimation as a sparse reconstruction problem. To this end, the proposed approach is derived to obtain the distribution of non-zero entries in a sparse channel. After that, the channel is reconstructed by utilizing the least-squares (LS) algorithm and compressed sensing (CS) theory. The simulation results demonstrate that the proposed channel estimation scheme is superior to existing solutions even in low signal-to-noise ratio (SNR) environments.

Keywords: channel estimation, reconfigurable intelligent surface, wireless communication, deep learning

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6837 Microalgae Hydrothermal Liquefaction Process Optimization and Comprehension to Produce High Quality Biofuel

Authors: Lucie Matricon, Anne Roubaud, Geert Haarlemmer, Christophe Geantet

Abstract:

Introduction: This case discusses the management of two floor of mouth (FOM) Squamous Cell Carcinomas (SCC) not identified upon initial biopsy. Case Report: A 51 year-old male presented with right FOM erythroleukoplakia. Relevant medical history included alcoholic dependence syndrome and alcoholic liver disease. Relevant drug therapy encompassed acamprosate, folic acid, hydroxocobalamin and thiamine. The patient had a 55.5 pack-year smoking history and alcohol dependence from age 14, drinking 16 units/day. FOM incisional biopsy and histopathological analysis diagnosed Carcinoma in situ. Treatment involved wide local excision. Specimen analysis revealed two separate foci of pT1 moderately differentiated SCCs. Carcinoma staging scans revealed no pathological lymphadenopathy, no local invasion or metastasis. SCCs had been excised in completion with narrow margins. MDT discussion concluded that in view of the field changes it would be difficult to identify specific areas needing further excision, although techniques such as Lugol’s Iodine were considered. Further surgical resection, surgical neck management and sentinel lymph node biopsy was offered. The patient declined intervention, primary management involved close monitoring alongside alcohol and smoking cessation referral. Discussion: Narrow excisional margins can increase carcinoma recurrence risk. Biopsy failed to identify SCCs, despite sampling an area of clinical concern. For gross field change multiple incisional biopsies should be considered to increase chance of accurate diagnosis and appropriate treatment. Coupling of tobacco and alcohol has a synergistic effect, exponentially increasing the relative risk of oral carcinoma development. Tobacco and alcoholic control is fundamental in reducing treatment‑related side effects, recurrence risk, and second primary cancer development.

Keywords: microalgae, biofuels, hydrothermal liquefaction, biomass

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6836 Hybrid Precoder Design Based on Iterative Hard Thresholding Algorithm for Millimeter Wave Multiple-Input-Multiple-Output Systems

Authors: Ameni Mejri, Moufida Hajjaj, Salem Hasnaoui, Ridha Bouallegue

Abstract:

The technology advances have most lately made the millimeter wave (mmWave) communication possible. Due to the huge amount of spectrum that is available in MmWave frequency bands, this promising candidate is considered as a key technology for the deployment of 5G cellular networks. In order to enhance system capacity and achieve spectral efficiency, very large antenna arrays are employed at mmWave systems by exploiting array gain. However, it has been shown that conventional beamforming strategies are not suitable for mmWave hardware implementation. Therefore, new features are required for mmWave cellular applications. Unlike traditional multiple-input-multiple-output (MIMO) systems for which only digital precoders are essential to accomplish precoding, MIMO technology seems to be different at mmWave because of digital precoding limitations. Moreover, precoding implements a greater number of radio frequency (RF) chains supporting more signal mixers and analog-to-digital converters. As RF chain cost and power consumption is increasing, we need to resort to another alternative. Although the hybrid precoding architecture has been regarded as the best solution based on a combination between a baseband precoder and an RF precoder, we still do not get the optimal design of hybrid precoders. According to the mapping strategies from RF chains to the different antenna elements, there are two main categories of hybrid precoding architecture. Given as a hybrid precoding sub-array architecture, the partially-connected structure reduces hardware complexity by using a less number of phase shifters, whereas it sacrifices some beamforming gain. In this paper, we treat the hybrid precoder design in mmWave MIMO systems as a problem of matrix factorization. Thus, we adopt the alternating minimization principle in order to solve the design problem. Further, we present our proposed algorithm for the partially-connected structure, which is based on the iterative hard thresholding method. Through simulation results, we show that our hybrid precoding algorithm provides significant performance gains over existing algorithms. We also show that the proposed approach reduces significantly the computational complexity. Furthermore, valuable design insights are provided when we use the proposed algorithm to make simulation comparisons between the hybrid precoding partially-connected structure and the fully-connected structure.

Keywords: alternating minimization, hybrid precoding, iterative hard thresholding, low-complexity, millimeter wave communication, partially-connected structure

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6835 Evaluation of Microstructure, Mechanical and Abrasive Wear Response of in situ TiC Particles Reinforced Zinc Aluminum Matrix Alloy Composites

Authors: Mohammad M. Khan, Pankaj Agarwal

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The present investigation deals with the microstructures, mechanical and detailed wear characteristics of in situ TiC particles reinforced zinc aluminum-based metal matrix composites. The composites have been synthesized by liquid metallurgy route using vortex technique. The composite was found to be harder than the matrix alloy due to high hardness of the dispersoid particles therein. The former was also lower in ultimate tensile strength and ductility as compared to the matrix alloy. This could be explained to be due to the use of coarser size dispersoid and larger interparticle spacing. Reasonably uniform distribution of the dispersoid phase in the alloy matrix and good interfacial bonding between the dispersoid and matrix was observed. The composite exhibited predominantly brittle mode of fracture with microcracking in the dispersoid phase indicating effective easy transfer of load from matrix to the dispersoid particles. To study the wear behavior of the samples three different types of tests were performed namely: (i) sliding wear tests using a pin on disc machine under dry condition, (ii) high stress (two-body) abrasive wear tests using different combinations of abrasive media and specimen surfaces under the conditions of varying abrasive size, traversal distance and load, and (iii) low-stress (three-body) abrasion tests using a rubber wheel abrasion tester at various loads and traversal distances using different abrasive media. In sliding wear test, significantly lower wear rates were observed in the case of base alloy over that of the composites. This has been attributed to the poor room temperature strength as a result of increased microcracking tendency of the composite over the matrix alloy. Wear surfaces of the composite revealed the presence of fragmented dispersoid particles and microcracking whereas the wear surface of matrix alloy was observed to be smooth with shallow grooves. During high-stress abrasion, the presence of the reinforcement offered increased resistance to the destructive action of the abrasive particles. Microcracking tendency was also enhanced because of the reinforcement in the matrix. The negative effect of the microcracking tendency was predominant by the abrasion resistance of the dispersoid. As a result, the composite attained improved wear resistance than the matrix alloy. The wear rate increased with load and abrasive size due to a larger depth of cut made by the abrasive medium. The wear surfaces revealed fine grooves, and damaged reinforcement particles while subsurface regions revealed limited plastic deformation and microcracking and fracturing of the dispersoid phase. During low-stress abrasion, the composite experienced significantly less wear rate than the matrix alloy irrespective of the test conditions. This could be explained to be due to wear resistance offered by the hard dispersoid phase thereby protecting the softer matrix against the destructive action of the abrasive medium. Abraded surfaces of the composite showed protrusion of dispersoid phase. The subsurface regions of the composites exhibited decohesion of the dispersoid phase along with its microcracking and limited plastic deformation in the vicinity of the abraded surfaces.

Keywords: abrasive wear, liquid metallurgy, metal martix composite, SEM

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6834 Field Evaluation of Fusarium Head Blight in Durum Wheat Caused by Fusarium culmorum in Algeria

Authors: Salah Hadjout, Mohamed Zouidi

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In Algeria, several works carried out in recent years have shown the importance of fusarium head blight in durum wheat. Indeed, this disease is caused by a complex of Fusarium genus pathogens. The research carried out reports that F. culmorum is the main species infecting cereals. These informations motivated our interest in the field evaluation of the behavior of some durum wheat genotypes (parental varieties and lines) with regard to fusarium head blight, mainly caused by four F. culmorum isolates. Our research work focused on following the evolution of symptom development throughout the grain filling, after artificial inoculation of ears by Fusarium isolates in order to establish a first image on the differences in genotype behavior to fusarium haed blight. Field disease assessment criteria are: disease assessment using a grading scale, thousand grain weight measurement and AUDPC. The results obtained revealed that the varieties and lines resulting from crosses had a quite different level of sensitivity to F. culmorum species and no genotype showed complete resistance in our culture conditions. Among the material tested, some lines showed higher resistance than their parents. The results also show a slight behavioral variability also linked to the aggressiveness of the Fusarium species studied in this work. Our results open very important research perspectives on fusarium head blight, in particular the search for toxins produced by Fusarium species.

Keywords: fusarium head blight, durum wheat, Fusarium culmorum, field disease assessment criteria, Algeria

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6833 Inhibition of Echis ocellatus Venom Metalloprotease by Flavonoid-Rich Ethyl Acetate Sub-fraction of Moringa oleifera Leaves (Lam.): in vitro and in silico Approaches

Authors: Adeyi Akindele Oluwatosin, Mustapha Kaosarat Keji, Ajisebiola Babafemi Siji, Adeyi Olubisi Esther, Damilohun Samuel Metibemu, Raphael Emuebie Okonji

Abstract:

Envenoming by Echis ocellatus is potentially life-threatening due to severe hemorrhage, renal failure, and capillary leakage. These effects are attributed to snake venom metalloproteinases (SVMPs). Due to drawbacks in the use of antivenom, natural inhibitors from plants are of interest in studies of new antivenom treatment. Antagonizing effects of bioactive compounds of Moringa oleifera, a known antisnake plant, are yet to be tested against SVMPs of E. ocellatus (SVMP-EO). Ethanol crude extract of M. oleifera was partitioned using n-hexane and ethyl acetate. Each partition was fractionated using column chromatography and tested against SVMP-EO purified through ion-exchange chromatography with EchiTab-PLUS polyvalent anti-venom as control. Phytoconstituents of ethyl acetate fraction were screened against the catalytic site of crystal of BaP1-SVMP, while drug-likeness and ADMET toxicity of compound were equally determined. The molecular weight of isolated SVMP-EO was 43.28 kDa, with a specific activity of 245 U/ml, a percentage yield of 62.83 %, and a purification fold of 0.920. The Vmax and Km values are 2 mg/ml and 38.095 μmol/ml/min, respectively, while the optimal pH and temperature are 6.0 and 40°C, respectively. Polyvalent anti-venom, crude extract, and ethyl acetate fraction of M. oleifera exhibited a complete inhibitory effect against SVMP-EO activity. The inhibitions of the P-1 and P-II metalloprotease’s enzymes by the ethyl acetate fraction are largely due to methanol, 6, 8, 9-trimethyl-4-(2-phenylethyl)-3-oxabicyclo[3.3.1]non-6-en-1-yl)- and paroxypropione, respectively. Both compounds are potential drug candidates with little or no concern of toxicity, as revealed from the in-silico predictions. The inhibitory effects suggest that this compound might be a therapeutic candidate for further exploration for treatment of Ocellatus’ envenoming.

Keywords: Echis ocellatus, Moringa oleifera, anti-venom, metalloproteases, snakebite, molecular docking

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6832 Bioavailability Enhancement of Ficus religiosa Extract by Solid Lipid Nanoparticles

Authors: Sanjay Singh, Karunanithi Priyanka, Ramoji Kosuru, Raju Prasad Sharma

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Herbal drugs are well known for their mixed pharmacological activities with the benefit of no harmful side effects. The use of herbal drugs is limited because of their higher dose requirement, frequent drug administration, poor bioavailability of phytochemicals and delayed onset of action. Ficus religiosa, a potent anti-oxidant plant useful in the treatment of diabetes and cancer was selected for the study. Solid lipid nanoparticles (SLN) of Ficus religiosa extract was developed for the enhancement in oral bioavailability of stigmasterol and β-sitosterol-d-glucoside, principal components present in the extract. Hot homogenization followed by ultrasonication method was used to develop extract loaded SLN. Developed extract loaded SLN were characterized for particle size, PDI, zeta potential, entrapment efficiency, in vitro drug release and kinetics, fourier transform infra-red spectroscopy, differential scanning calorimetry, powder X-ray diffractrometry and stability studies. Entrapment efficiency of optimized extract loaded SLN was found to be 68.46 % (56.13 % of stigmasterol and 12.33 % of β-sitosteryl-d-glucoside, respectively). RP HPLC method development was done for simultaneous estimation of stigmasterol and β-sitosterol-d-glucoside in Ficus religiosa extract in rat plasma. Bioavailability studies were carried out for extract in suspension form and optimized extract loaded SLN. AUC of stigmasterol and β-sitosterol-d-glucoside were increased by 6.7-folds by 9.2-folds, respectively in rats treated with extract loaded SLN compared to extract suspension. Also, Cmax of stigmasterol and β-sitosterol-d-glucoside were increased by 4.3-folds by 3.9-folds, respectively in rats treated with extract loaded SLN compared to extract suspension. Mean residence times (MRT) for stigmasterol were found to be 12.3 ± 0.67 hours from extract and 7.4 ± 2.1 hours from SLN and for β-sitosterol-d-glucoside, 10.49 ± 2.9 hours from extract and 6.4 ± 0.3 hours from SLN. Hence, it was concluded that SLN enhanced the bioavailability and reduced the MRT of stigmasterol and β-sitosterol-d-glucoside in Ficus religiosa extract which in turn may lead to reduction in dose of Ficus religiosa extract, prolonged duration of action and also enhanced therapeutic efficacy.

Keywords: Ficus religiosa, phytosterolins, bioavailability, solid lipid nanoparticles, stigmasterol and β-sitosteryl-d-glucoside

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