Search results for: formic acid fuel cell
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Search results for: formic acid fuel cell

1729 Designing, Preparation and Structural Evaluation of Co-Crystals of Oxaprozin

Authors: Maninderjeet K. Grewal, Sakshi Bhatnor, Renu Chadha

Abstract:

The composition of pharmaceutical entities and the molecular interactions can be altered to optimize drug properties such as solubility and bioavailability by the crystal engineering technique. The present work has emphasized on the preparation, characterization, and biopharmaceutical evaluation of co-crystal of BCS Class II anti-osteoarthritis drug, Oxaprozin (OXA) with aspartic acid (ASPA) as co-former. The co-crystals were prepared through the mechanochemical solvent drop grinding method. Characterization of the prepared co-crystal (OXA-ASPA) was done by using analytical tools such as differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FT-IR), powder X-ray diffraction (PXRD). DSC thermogram of OXA-ASPA cocrystal showed a single sharp melting endotherm at 235 ºC, which was between the melting peaks of the drug and the counter molecules suggesting the formation of a new phase which is a co-crystal that was further confirmed by using other analytical techniques. FT-IR analysis of OXA-ASPA cocrystal showed a shift in a hydroxyl, carbonyl, and amine peaks as compared to pure drugs indicating all these functional groups are participating in cocrystal formation. The appearance of new peaks in the PXRD pattern of cocrystals in comparison to individual components showed that a new crystalline entity has been formed. The Crystal structure of cocrystal was determined using material studio software (Biovia) from PXRD. The equilibrium solubility study of OXA-ASPA showed improvement in solubility as compared to pure drug. Therefore, it was envisioned to prepare the co-crystal of oxaprozin with a suitable conformer to modulate its physiochemical properties and consequently, the biopharmaceutical parameters.

Keywords: cocrystals, coformer, oxaprozin, solubility

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1728 Wound Healing Potential and Comparison of Mummy Substance Effect on Adipose and Wharton’s Jelly-Derived Mesenchymal Stem Cells Co-Cultured with Human Fibroblast

Authors: Sepideh Hassanpour Khodaei

Abstract:

Background/Objectives: The purpose of this study is to evaluate the effect of mummy substances on two issues of proliferation and production of matrix protein synthesis in wound healing. Methods: The methodology used for this aim involves isolating mesenchymal stem cells and human fibroblasts procured at Pastor Institute, Iran. The cells were treated with mummy substances separately and co-cultured between ASCs and WJSCs, and fibroblasts. Proliferation was assessed by Ki67 method in monolayer conditions. Synthesis of components of extracellular matrix (ECM) such as collagen type I, type III, and fibronectin 1 (FN1) was determined by qPCR. Results: The effects of adipocyte stem cells (ASCs), Wharton Jelly Stem Cells (WJSCs), and Mummy material on fibroblast proliferation and migration were evaluated. The present finding underlined the importance of Mummy material, ASCs, and WJSCs in the proliferation and migration of fibroblast cells. Furthermore, the expression of collagen I, III, and FN1 was increased in the presence of the above material and cells. Conclusion: This study presented an effective in vitro method for the healing process. Hence, the prospect of utilizing Mummy material and stem cell-based therapies in wound healing as a therapeutic approach is promising.

Keywords: mummy material, wound healing, adipose tissue, Wharton’s jelly

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1727 In vitro Inhibitory Action of an Aqueous Extract of Carob on the Release of Myeloperoxidase by Human Neutrophils

Authors: Kais Rtibi, Slimen Selmi, Jamel El-Benna, Lamjed Marzouki, Hichem Sebai

Abstract:

Background: Myeloperoxidase (MPO) is a hemic enzyme found in high concentrations in the primary neutrophils granules. In addition to its peroxidase activity, it has a chlorination activity, using hydrogen peroxide and chloride ions to form hypochlorous acid, a strong oxidant, capable of chlorinating molecules. Bioactive compounds contained in medicinal plants could limit the action of this enzyme to reduce the reactive oxygen species production and its chlorination activity. The purpose of this study is to evaluate the effect of the carob aqueous extract (CAE) on the release of MPO by human neutrophils in vitro and its activity following stimulation of these cells by PMA. Methods: Neutrophils were isolated by simple sedimentation using the Dextran/Ficoll method. After stimulation with phorbol 12-myristate 13-acetate (PMA), neutrophils release the MPO by degranulation. The effect of CAE on the release of MPO was analyzed by the Western blot technique, while, its activity was determined by biochemical method using the method of 3,3', 5,5'- Tetramethylbenzidine (TMB) and hydrogen peroxide. The data were expressed as mean ± SEM. Results: The carob aqueous extract causes a decrease in MPO quantity and activity in a concentration-dependent manner which leads to a reduction of the production of the ROS (reactive oxygen species) and the protection of the molecules against oxidation and chlorination mechanisms. Conclusion: Thanks to its richness in bioactive compounds, the aqueous extract of carob could limit the development of damages related to the uncontrolled activity of MPO.

Keywords: carob, MPO, myeloperoxidase, neutrophils, PMA, phorbol 12-myristate 13-acetate

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1726 Parkinson’s Disease Detection Analysis through Machine Learning Approaches

Authors: Muhtasim Shafi Kader, Fizar Ahmed, Annesha Acharjee

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Machine learning and data mining are crucial in health care, as well as medical information and detection. Machine learning approaches are now being utilized to improve awareness of a variety of critical health issues, including diabetes detection, neuron cell tumor diagnosis, COVID 19 identification, and so on. Parkinson’s disease is basically a disease for our senior citizens in Bangladesh. Parkinson's Disease indications often seem progressive and get worst with time. People got affected trouble walking and communicating with the condition advances. Patients can also have psychological and social vagaries, nap problems, hopelessness, reminiscence loss, and weariness. Parkinson's disease can happen in both men and women. Though men are affected by the illness at a proportion that is around partial of them are women. In this research, we have to get out the accurate ML algorithm to find out the disease with a predictable dataset and the model of the following machine learning classifiers. Therefore, nine ML classifiers are secondhand to portion study to use machine learning approaches like as follows, Naive Bayes, Adaptive Boosting, Bagging Classifier, Decision Tree Classifier, Random Forest classifier, XBG Classifier, K Nearest Neighbor Classifier, Support Vector Machine Classifier, and Gradient Boosting Classifier are used.

Keywords: naive bayes, adaptive boosting, bagging classifier, decision tree classifier, random forest classifier, XBG classifier, k nearest neighbor classifier, support vector classifier, gradient boosting classifier

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1725 High Efficacy of Combined Therapy with Microbicide BASANT and Triple Combination of Selected Probiotics for Treatment of Vaginosis and Restoration of Vaginal Health

Authors: Nishu Atrey, Priyanka Singh, G. P. Talwar, Jagdish Gupta, Alka Kriplani, Rohini Sehgal, Indrani Ganguli, Soni Sinha

Abstract:

Background: Vaginosis is a widely prevalent syndrome in India and elsewhere. Recurrence is frequent in women treated with antibiotics, whose vagina pH remains above 5.0 indicative of the loss of resident lactobacilli. The objective of the present trial was to determine whether a Polyherbal microbicide BASANT can regress Vaginosis. Another objective was to determine whether the three selected strains of Probiotics endowed with making high amounts of lactic acid can colonise and restore the pH of the vagina to the acidic healthy range. Materials and Procedure: BASANT, was employed in powder form in veg (cellulose) capsules. TRF#36 strain of Lactobacillus fermentum, TRF#8 strain of L.gasseri, and TRF#30 strain of L.salivarius (combination termed as Pro-vag-Health) were employed at 3x109 bacilli lyophilized, packaged in capsules. The trials were conducted in women suffering from vaginosis with vaginal pH above 5.0. Women were given intravaginally either BASANT, Pro-vag-Health or a combination of the two intravaginally for seven days and thereafter once weekly as a maintenance dose. Results: BASANT cleared vaginosis in 14/20 women and Pro-vag-Health in 13/20 women. Interestingly, the combination of BASANT plus Pro-vag-Health was effective in 19/20 women, in contrast to Placebo capsules effective only in 1/20 women. Interpretation and Conclusion: The combination of BASANT and Pro-veg-Health Probiotics taken together intravaginally for seven days relieves 19 out of 20 women from vaginosis to restore acidic pH and healthy vagina. Extension of trial with this combination in larger number is indicated.

Keywords: microbicide, probiotics, vaginal pH, vaginosis

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1724 Effects of Drying Temperatures on the Qualitative and Quantitative Phytochemicals of Aqueous Extracts If the Calyces of Hibiscus Sabdariffa

Authors: John O. Efosa, S. Egielewa, M. A. Azeke

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Hibiscus sabdariffa (Hs) is known for its delicacy and also for medicinal properties. The flower calyces are usually sun- or oven-dried after harvesting. There are unverified claims that calyces dried at lower temperatures have better medicinal potentials than those dried at higher temperatures. The present work, therefore, aimed to study the effects of drying temperatures on the photochemical composition and antioxidant potential of aqueous extracts of the calyces of Hs. The calyces were dried at different temperatures (freeze-drying at -580C, drying at 300C, 400C, and 500 C.) respectively to constant weight. Samples (25 g) of dried calyces from each drying temperatures were weighed and placed in clean conical flasks and extracted; each was used for the analysis. Validated analytical assays were used for the determination of the different Phytochemicals. From the results obtained, it was observed that drying at 30°C resulted in the highest retention of total phenols, total flavonoids, tannins, alkaloids and saponins. Using the Inhibition Concentration values (IC50), some antioxidant parameters were found to follow the same trend as the earlier mentioned phytochemicals. Drying at 30°C resulted in the highest retention of DPPH Radical Scavenging Activity, Ferric Reducing Antioxidant Potential (FRAP), Nitrite radical scavenging Activity, 2, 2-azinobis-3-ethylbenzotiazoline-6-sulfonic acid (ABTS) radical scavenging activity There were, however, significant reductions in vitamin C and oxalate contents as the drying temperature increased (P < 0.05). From the results, it recommended that the calyces of Hibiscus sabdariffa be dried at 30°C in order to optimally elicit its medicinal potentials.

Keywords: antioxidant, drying temperature, hibiscus sabdariffa, phytochemicals, quantitative

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1723 Biodegradable Polymer Film Incorporated with Polyphenols for Active Packaging

Authors: Shubham Sharma, Swarna Jaiswal, Brendan Duffy, Amit Jaiswal

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The key features of any active packaging film are its biodegradability and antimicrobial properties. Biological macromolecules such as polyphenols (ferulic acid (FA) and tannic acids (TA)) are naturally found in plants such as grapes, berries, and tea. In this study, antimicrobial activity screening of several polyphenols was carried out by using minimal inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) against two strains of gram-negative bacteria - Salmonella typhimurium, Escherichia coli, and two-gram positive strains - Staphylococcus aureus and Listeria monocytogenes. FA and TA had shown strong antibacterial activity at the low concentration against both gram-positive and gram-negative bacteria. The selected polyphenols FA and TA were incorporated at various concentrations (1%, 5%, and 10% w/w) in the poly(lactide) – poly (butylene adipate-co-terephthalate) (PLA-PBAT) composite film by using the solvent casting method. The effect of TA and FA incorporation in the packaging was characterized based on morphological, optical, color, mechanical, thermal, and antimicrobial properties. The thickness of the FA composite film was increased by 1.5 – 7.2%, while for TA composite film, it increased by 0.018 – 1.6%. FA and TA (10 wt%) composite film had shown approximately 65% - 66% increase in the UV barrier property. As the FA and TA concentration increases from 1% - 10% (w/w), the TS value increases by 1.98 and 1.80 times, respectively. The water contact angle of the film was observed to decrease significantly with the increase in the FA and TA content in the composite film. FA has shown more significant increase in antimicrobial activity than TA in the composite film against Listeria monocytogenes and E. coli. The FA and TA composite film has the potential for its application as an active food packaging.

Keywords: active packaging, biodegradable film, polyphenols, UV barrier, tensile strength

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1722 Intermittent Effect of Coupled Thermal and Acoustic Sources on Combustion: A Spatial Perspective

Authors: Pallavi Gajjar, Vinayak Malhotra

Abstract:

Rockets have been known to have played a predominant role in spacecraft propulsion. The quintessential aspect of combustion-related requirements of a rocket engine is the minimization of the surrounding risks/hazards. Over time, it has become imperative to understand the combustion rate variation in presence of external energy source(s). Rocket propulsion represents a special domain of chemical propulsion assisted by high speed flows in presence of acoustics and thermal source(s). Jet noise leads to a significant loss of resources and every year a huge amount of financial aid is spent to prevent it. External heat source(s) induce high possibility of fire risk/hazards which can sufficiently endanger the operation of a space vehicle. Appreciable work had been done with justifiable simplification and emphasis on the linear variation of external energy source(s), which yields good physical insight but does not cater to accurate predictions. Present work experimentally attempts to understand the correlation between inter-energy conversions with the non-linear placement of external energy source(s). The work is motivated by the need to have better fire safety and enhanced combustion. The specific objectives of the work are a) To interpret the related energy transfer for combustion in presence of alternate external energy source(s) viz., thermal and acoustic, b) To fundamentally understand the role of key controlling parameters viz., separation distance, the number of the source(s), selected configurations and their non-linear variation to resemble real-life cases. An experimental setup was prepared using incense sticks as potential fuel and paraffin wax candles as the external energy source(s). The acoustics was generated using frequency generator, and source(s) were placed at selected locations. Non-equidistant parametric experimentation was carried out, and the effects were noted on regression rate changes. The results are expected to be very helpful in offering a new perspective into futuristic rocket designs and safety.

Keywords: combustion, acoustic energy, external energy sources, regression rate

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1721 Effects of Porcine Oviductal Fluid on In vitro Growth of Dendrobium mirbelianum

Authors: M. Youngsabanant-Areekijseree, C. Thepsithar, K. Sribuddhachart, J. Tananantayot

Abstract:

Porcine oviductal fluid (pOF) from oviduct, an unused organ from the slaughterhouse, was effectively used for biotechnology studies. The fluid components consisted of micro- and macro-nutrients, amino acids, carbon source and proteins that played important roles in animal cell and embryo development. This was our knowledge on investigating pOF as growth promoting substance in culture medium of an orchid, Dendrobium mirbelianum. Two-leaf shoots were cultured in liquid Vacin and Went (VW) medium as a standard medium supplemented with 2 g/L peptone (Pe) or 100 g/ L boiled-potato water (Po) alone or in combinations, and added with 0, 1, 3 or 5 ml/L pOF. All explants were cultured in a stationary condition for 8 weeks. It was found that medium added with 100 g/L Po and 1 ml/L pOF provided the best results (1.02 g fresh weight, 4.2 shoots, 0.53 cm shoot height, 4.4 protocorms, 11.0 leaves and 5.7 roots with 100% survival) when compared to other medium, but not statistically significant difference from medium added with 100 g/L Po (0.86 g fresh weight, 4.3 shoots, 0.51 cm shoot height, 4.6 protocorms, 12.4 leaves and 6.6 roots with 100% survival). However, VW medium supplemented with 1 or 3 ml/L pOF alone showed the higher percentage of survival (100%) than VW medium (86.67%). It was shown the potential role of pOF as an organic supplement for promoting growth of plants. Acknowledgements—The project was funded by a grant from Silpakorn University Research & Development Institute (SURDI) and Faculty of Science, Silpakorn University, Thailand.

Keywords: Dendrobium mirbelianum, pig, oviductal fluid, in vitro growth

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1720 Use of Amaranthus Roxburghianus Root Extract in the Treatment of Ulcerative Colitis in Mice

Authors: S. A. Nirmal, J. M. Ingale, G. S. Asane, S. C. Pal, Subhash C. Mandal

Abstract:

The present work was undertaken to determine the effects of Amaranthus roxburghianus Nevski. (Amaranthaceae) root alone and in combination with piperine in treating ulcerative colitis (UC) in mice. Swiss albino mice were divided into seven groups (n = 6). Standard group received prednisolone (5 mg/kg, i.p.). Treatment groups received hydroalcoholic extract of roots of A. roxburghianus (50 and 100 mg/kg, p.o.) and a combination of hydroalcoholic extract of roots of A. roxburghianus (50 and 100 mg/kg, p.o.) and piperine (5 mg/kg, p.o.). Ulcer index, colitis severity, myeloperoxidase (MPO), malondialdehyde and glutathione were estimated from blood and tissue. Column chromatography of the extract was done and purified fractions were analyzed by gas chromatography-mass spectroscopy (GC-MS). Treatment with the combination of hydroalcoholic extract of A. roxburghianus and piperine showed minimal ulceration, hemorrhage, necrosis and leucocyte infiltration by histopathological observation. Acetic acid increased MPO levels in blood and colon tissue to 355 U/mL and 385 U/mg, respectively. The combination of hydroalcoholic extract (100 mg/kg) and piperine (5 mg/kg) significantly decreased MPO in blood and tissue to 182 U/mL and 193 U/mg, respectively. Similarly, this combination significantly reduced MPO and increased glutathione levels in blood and tissue. Various phytoconstituents were detected by GC-MS. The combination of hydroalcoholic extract and piperine is effective in the treatment of UC and the effects are comparable with the standard drug prednisolone. 4H-pyran-4-one, 2,3-dihydro-3,5-dihydroxy-6-methyl, eugenol and benzene, and 1-(1,5-dimethyl-4-hexenyl)-4-methyl are reported having analgesic, anti-inflammatory, and antioxidant properties; they may play a role in the biological activity of A. roxburghianus root.

Keywords: Amaranthus roxburghianus, ulcerative colitis, anti-inflammatory, ulcerative colitis

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1719 Wheat (Triticum Aestivum) Yield Improved with Irrigation Scheduling under Salinity

Authors: Taramani Yadav, Gajender Kumar, R.K. Yadav, H.S. Jat

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Soil Salinity and irrigation water salinity is critical threat to enhance agricultural food production to full fill the demand of billion plus people worldwide. Salt affected soils covers 6.73 Mha in India and ~1000 Mha area around the world. Irrigation scheduling of saline water is the way to ensure food security in salt affected areas. Research experiment was conducted at ICAR-Central Soil Salinity Research Institute, Experimental Farm, Nain, Haryana, India with 36 treatment combinations in double split plot design. Three sets of treatments consisted of (i) three regimes of irrigation viz., 60, 80 and 100% (I1, I2 and I3, respectively) of crop ETc (crop evapotranspiration at identified respective stages) in main plot; (ii) four levels of irrigation water salinity (sub plot treatments) viz., 2, 4, 8 and 12 dS m-1 (iii) applications of two PBRs along with control (without PBRs) i.e. salicylic acid (G1; 1 mM) and thiourea (G2; 500 ppm) as sub-sub plot treatments. Grain yield of wheat (Triticum aestivum) was increased with less amount of high salt loaded irrigation water at the same level of salinity (2 dS m-1), the trend was I3>I2>I1 at 2 dS m-1 with 8.10 and 17.07% increase at 80 and 100% ETc, respectively compared to 60% ETc. But contrary results were obtained by increasing amount of irrigation water at same level of highest salinity (12 dS m-1) showing following trend; I1>I2>I3 at 12 dS m-1 with 9.35 and 12.26% increase at 80 and 60% ETc compared to 100% ETc. Enhancement in grain yield of wheat (Triticum aestivum) is not need to increase amount of irrigation water under saline condition, with salty irrigation water less amount of irrigation water gave the maximum wheat (Triticum aestivum) grain yield.

Keywords: Irrigation, Salinity, Wheat, Yield

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1718 Effects of Rising Cost of Building Materials in Nigeria: A Case Study of Adamawa State

Authors: Ibrahim Yerima Gwalem, Jamila Ahmed Buhari

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In recent years, there has been an alarming rate of increase in the costs of building materials in Nigeria, and this ugly phenomenon threatens the contributions of the construction industry in national development. The purpose of this study was to assess the effects of the rising cost of building materials in Adamawa State Nigeria. Four research questions in line with the purpose of the study were raised to guide the study. Two null hypotheses were formulated and tested at 0.05 level of significance. The study adopted a survey research design. The population of the study comprises registered contractors, registered builders, selected merchants, and consultants in Adamawa state. Data were collected using researcher designed instrument tagged effects of the rising cost of building materials questionnaire (ERCBMQ). The instrument was subjected to face and content validation by two experts, one from Modibbo Adama University of Technology Yola and the other from Federal Polytechnic Mubi. The reliability of the instrument was determined by the Cronbach Alpha method and yielded a reliability index of 0.85 high enough to ascertain the reliability. Data collected from a field survey of 2019 was analyzed using mean and percentage. The means of the prices were used in the calculations of price indices and rates of inflation on building materials. Findings revealed that factors responsible for the rising cost of building materials are the exchange rate of the Nigeria Naira with a mean rating (MR) = 4.4; cost of fuel and power supply, MR = 4.3; and changes in government policies and legislation, MR = 4.2, while fluctuations in the construction cost with MR = 2.8; reduced volume of construction output, MR = 2.52; and risk of project abandonment, MRA = 2.51, were the three effects. The study concluded that adverse effects could result in a downward effect on the contributions of the construction industries on the gross domestic product (GDP) in the nation’s economy. Among the recommendations proffered include that the government should formulate a policy that will play down the agitations on the use of imported building materials by encouraging research in the production of local building materials.

Keywords: effects, rising, cost, building, materials

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1717 Carbon Aerogel Spheres from Resorcinol/Phenol and Formaldehyde for CO₂ Adsorption

Authors: Jessica Carolina Hernandez Galeano, Juan Carlos Moreno Pirajan, Liliana Giraldo

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Carbon gels are materials whose structure and porous texture can be designed and controlled on a nanoscale. Among their characteristics it is found their low density, large surface area and high degree of porosity. These materials are produced by a sol-gel polymerization of organic monomers using basic or acid catalysts, followed by drying and controlled carbonization. In this work, the synthesis and characterization of carbon aerogels from resorcinol, phenol and formaldehyde in ethanol is described. The aim of this study is obtaining different carbonaceous materials in the form of spheres using the Stöber method to perform a further evaluation of CO₂ adsorption of each material. In general, the synthesis consisted of a sol-gel polymerization process that generates a cluster (cross-linked organic monomers) from the precursors in the presence of NH₃ as a catalyst. This cluster was subjected to specific conditions of gelling and curing (30°C for 24 hours and 100°C for 24 hours, respectively) and CO₂ supercritical drying. Finally, the dry material was subjected to a process of carbonization or pyrolysis, in N₂ atmosphere at 350°C (1° C / min) for 2 h and 600°C (1°C / min) for 4 hours, to obtain porous solids that retain the structure initially desired. For this work, both the concentrations of the precursors and the proportion of ammonia in the medium where modify to describe the effect of the use of phenol and the amount of catalyst in the resulting material. Carbon aerogels were characterized by Scanning Electron Microscope (SEM), N₂ isotherms, infrared spectroscopy (IR) and X-ray Powder Diffraction (XRD) showing the obtention of carbon spheres in the nanometric scale with BET areas around 500 m2g-1.

Keywords: carbon aerogels, carbon spheres, CO₂ adsorption, Stöber method

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1716 Effect of Different Levels of Dried Citrus Sinensis Peel on Blood Parameters of Broilers

Authors: Abbas Ebrahimi, Zohreh Pourhossein, Nariman Miraalami

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The experiment was conducted to evaluate the effects of different levels of dried citrus sinensis peel (DCSP) on the blood parameters of broilers. Four hundred Ross 308 strain day old broiler in a completely randomized design with five treatments (four replicates per treatment and each replicate had 20 chicks) were categorized. Each treatment used either regulatory diet including 1.5% and 3% DCSP in the base diet and in two periods of 1st to 21st day and 1st to 42nd day and base diet without any additive for six weeks. Data analysis was performed using SAS software and mean comparison was conducted by Duncan method. The results determined that using different level of DCSP has significant effects on blood plasma parameters (P<0.05). Cholesterol, glucose, triglyceride, low density lipoprotein (LDL) at the rearing period was significantly influenced by experimental treatments (P<0.05). However, uric acid, alkaline phosphatase and high density lipoprotein (HDL) was not affected by experimental treatments (P>0.05). The lowest rate of blood cholesterol was concerned to the treatment which was used 3% DCSP 1st to 42nd day and the highest mean of blood cholesterol were concerned to the control treatment. The lowest rate of blood triglyceride was concerned to the treatment which was used 3% DCSP 1st to 42nd day and the highest mean of blood triglyceride were concerned to the control treatment. The lowest rate of blood alkaline phosphatase was concerned to the treatment which was used 3% DCSP 1st to 42nd day and the highest mean of blood alkaline phosphatase were concerned to the treatment which was used 3% DCSP 1st to 21st day.

Keywords: blood parameters, broilers, dried citrus sinensis peel, regulatory diet

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1715 Information Management Approach in the Prediction of Acute Appendicitis

Authors: Ahmad Shahin, Walid Moudani, Ali Bekraki

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This research aims at presenting a predictive data mining model to handle an accurate diagnosis of acute appendicitis with patients for the purpose of maximizing the health service quality, minimizing morbidity/mortality, and reducing cost. However, acute appendicitis is the most common disease which requires timely accurate diagnosis and needs surgical intervention. Although the treatment of acute appendicitis is simple and straightforward, its diagnosis is still difficult because no single sign, symptom, laboratory or image examination accurately confirms the diagnosis of acute appendicitis in all cases. This contributes in increasing morbidity and negative appendectomy. In this study, the authors propose to generate an accurate model in prediction of patients with acute appendicitis which is based, firstly, on the segmentation technique associated to ABC algorithm to segment the patients; secondly, on applying fuzzy logic to process the massive volume of heterogeneous and noisy data (age, sex, fever, white blood cell, neutrophilia, CRP, urine, ultrasound, CT, appendectomy, etc.) in order to express knowledge and analyze the relationships among data in a comprehensive manner; and thirdly, on applying dynamic programming technique to reduce the number of data attributes. The proposed model is evaluated based on a set of benchmark techniques and even on a set of benchmark classification problems of osteoporosis, diabetes and heart obtained from the UCI data and other data sources.

Keywords: healthcare management, acute appendicitis, data mining, classification, decision tree

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1714 Ethnopharmacological Analysis of Fermented Herbal Concoctions

Authors: Ishmael Ntlhamu

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In Limpopo Province, the use of herbal concoctions is becoming very popular. These concoctions are claimed to be capable of treating ulcers, diabetes, certain STDs, blood cleansing, and many more types of diseases. The aim of this study was to evaluate the phytochemical composition, evaluate the pharmacological effects and consumption safety in herbal concoctions to treat various kinds of ailments in Limpopo. The concoctions were extracted with 80% acetone. Microorganisms in the concoctions were identified using the Vitek 2 compact system. Qualitative phytochemical analysis was determined using standard chemical tests and thin layer chromatography (TLC). Total polyphenol content was quantified. Antioxidant activity was quantified using 2, 2-diphenyl-1-picrylhydrazyl (DPPH) assay and ferric reducing power. Antimicrobial activities were determined using a broth micro-dilution assay and bioautography. Cell viability assay was used to determine the cytotoxicity. Results showed that concoctions had antioxidant activity. Presence of different phytoconstituents was observed. Isolated microorganisms were identified as Burkholderia pseudomallei, Staphylococcus vitulimus, Enterococcus columbae, Kocuria kristanae, Staphylococcus intermedius, Cryptococcus laurenti. and Burkholderia pseudomallei (highly pathogenic). Therefore, phytochemicals prove that the concoctions can heal as the antimicrobial tests also displayed activity. Moreover, the concoctions did not exhibit cytotoxic effects. However, contaminants raise concerns, not only for consumer safety but also the quality of herbal concoctions available as part of the traditional medicinal practice in Limpopo.

Keywords: antimicrobials, concoctions, cytotoxicity, phytochemicals

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1713 The Relationship between First-Day Body Temperature and Mortality in Traumatic Patients

Authors: Neda Valizadeh, Mani Mofidi, Sama Haghighi, Ali Hashemaghaee, Soudabeh Shafiee Ardestani

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Background: There are many systems and parameters to evaluate trauma patients in the emergency department. Most of these evaluations are to distinguish patients with worse conditions so that the care systems have a better prediction of condition for a better care-giving. The purpose of this study is to determine the relationship between axillary body temperature and mortality in patients hospitalized in the intensive care unit (ICU) with multiple traumas and with other clinical and para-clinical factors. Methods: All patients between 16 and 75 years old with multiple traumas who were admitted into Emergency Department then hospitalized in the ICU were included in our study. An axillary temperature in the first and the second day of admission, Glasgow cola scale (GCS), systolic blood pressure, Serum glucose levels, and white blood cell counts of all patients at the admission day were recorded and their relationship with mortality were analyzed by SPSS software with suitable statistical tests. Results: Axillary body temperatures in the first and second day were statistically lower in expired traumatic patients (p=0.001 and p<0,001 respectively). Patients with lower GCS had a significantly lower first-day temperature and a significantly higher mortality. (p=0.006 and p=0.006 respectively). Furthermore, the first-day axillary temperature was significantly lower in patients with a lower first-day systolic blood pressure (p=0.014). Conclusion: Our results showed that lower axillary body temperature in the first day is associated with higher mortality, lower GCS, and lower systolic blood pressure. Thus, this could be used as a predictor of mortality in evaluation of traumatic patients in emergency settings.

Keywords: fever, trauma, mortality, emergency

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1712 Screening Deformed Red Blood Cells Irradiated by Ionizing Radiations Using Windowed Fourier Transform

Authors: Dahi Ghareab Abdelsalam Ibrahim, R. H. Bakr

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Ionizing radiation, such as gamma radiation and X-rays, has many applications in medical diagnoses and cancer treatment. In this paper, we used the windowed Fourier transform to extract the complex image of the deformed red blood cells. The real values of the complex image are used to extract the best fitting of the deformed cell boundary. Male albino rats are irradiated by γ-rays from ⁶⁰Co. The male albino rats are anesthetized with ether, and then blood samples are collected from the eye vein by heparinized capillary tubes for studying the radiation-damaging effect in-vivo by the proposed windowed Fourier transform. The peripheral blood films are prepared according to the Brown method. The peripheral blood film is photographed by using an Automatic Image Contour Analysis system (SAMICA) from ELBEK-Bildanalyse GmbH, Siegen, Germany. The SAMICA system is provided with an electronic camera connected to a computer through a built-in interface card, and the image can be magnified up to 1200 times and displayed by the computer. The images of the peripheral blood films are then analyzed by the windowed Fourier transform method to extract the precise deformation from the best fitting. Based on accurate deformation evaluation of the red blood cells, diseases can be diagnosed in their primary stages.

Keywords: windowed Fourier transform, red blood cells, phase wrapping, Image processing

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1711 In silico Analysis of a Causative Mutation in Cadherin-23 Gene Identified in an Omani Family with Hearing Loss

Authors: Mohammed N. Al Kindi, Mazin Al Khabouri, Khalsa Al Lamki, Tommasso Pappuci, Giovani Romeo, Nadia Al Wardy

Abstract:

Hereditary hearing loss is a heterogeneous group of complex disorders with an overall incidence of one in every five hundred newborns presented as syndromic and non-syndromic forms. Cadherin-related 23 (CDH23) is one of the listed deafness causative genes. CDH23 is found to be expressed in the stereocilia of hair cells and the retina photoreceptor cells. Defective CDH23 has been associated mostly with prelingual severe-to-profound sensorineural hearing loss (SNHL) in either syndromic (USH1D) or non-syndromic SNHL (DFNB12). An Omani family diagnosed clinically with severe-profound sensorineural hearing loss was genetically analysed by whole exome sequencing technique. A novel homozygous missense variant, c.A7451C (p.D2484A), in exon 53 of CDH23 was detected. One hundred and thirty control samples were analysed where all were negative for the detected variant. The variant was analysed in silico for pathogenicity verification using several mutation prediction software. The variant proved to be a pathogenic mutation and is reported for the first time in Oman and worldwide. It is concluded that in silico mutation prediction analysis might be used as a useful molecular diagnostics tool benefiting both genetic counseling and mutation verification. The aspartic acid 2484 alanine missense substitution might be the main disease-causing mutation that damages CDH23 function and could be used as a genetic hearing loss marker for this particular Omani family.

Keywords: Cdh23, d2484a, in silico, Oman

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1710 Antibiotic Prescribing Pattern and Associated Risk Factors Promoting Antibiotic Resistance, a Cross Sectional Study in a Regional Hospital in Ghana

Authors: Nicholas Agyepong, Paul Gyan

Abstract:

Inappropriate prescribing of antibiotic is a common healthcare concern globally resulted in an increased risk of adverse reactions and the emergence of antimicrobial resistance. The wrong antibiotic prescribing habits may lead to ineffective and unsafe treatment, worsening of disease condition, and thus increase in health care costs. The study was to examine the antibiotic prescribing pattern and associated risk factors at Regional Hospital in the Bono region of Ghana. A retrospective cross-sectional study was conducted to describe the current prescribing practices at the Hospital from January 2014 to December, 2021. A systematic random sampling method was used to select the participants for the study. STATA version 16 software was used for data management and analysis. Descriptive statistics and logistic regression analysis were used to analyze the data. Statistical significance set at p<0.05. Antibiotic consumption was equivalent to 11 per 1000 inhabitants consuming 1 DDD per day. Most common prescribed antibiotic was amoxicillin/clavulanic acid (14.39%) followed by erythromycin (11.44%), and ciprofloxacin (11.36%). Antibiotics prescription have been steadily increased over the past eight years (2014: n=59,280 to 2021: n=190,320). Prescribers above the age of 35 were more likely to prescribe antibiotics than those between the ages of 20 and 25 (COR=21.00; 95% CI: 1.78 – 48.10; p=0.016). Prescribers with at least 6 years of experience were also significantly more likely to prescribe antibiotics than those with at most 5 years of experience (COR=14.17; 95% CI: 2.39 – 84.07; p=0.004). Thus, the establishment of an antibiotic stewardship program in the hospitals is imperative, and further studies need to be conducted in other facilities to establish the national antibiotic prescription guideline.

Keywords: antibiotic, antimicrobial resistance, prescription, prescribers

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1709 Antibacterial Activity and Cytotoxicity of Silver Nanoparticles Synthesized by Moringa oleifera Extract as Reducing Agent

Authors: Temsiri Suwan, Penpicha Wanachantararak, Sakornrat Khongkhunthian, Siriporn Okonogi

Abstract:

In the present study, silver nanoparticles (AgNPs) were synthesized by green synthesis approach using Moringa oleifera aqueous extract (ME) as a reducing agent and silver nitrate as a precursor. The obtained AgNPs were characterized using UV-Vis spectroscopy (UV-Vis), dynamic light scattering (DLS), scanning electron microscopy (SEM), energy-dispersive X-ray spectroscopy (EDX), and X-ray diffractometry (XRD). The results from UV-Vis revealed that the maximum absorption of AgNPs was at 430 nm and the EDX spectrum confirmed Ag element. The results from DLS indicated that the amount of ME played an important role in particle size, size distribution, and zeta potential of the obtained AgNPs. The smallest size (62.4 ± 1.8 nm) with narrow distribution (0.18 ± 0.02) of AgNPs was obtained after using 1% w/v of ME. This system gave high negative zeta potential of -36.5 ± 2.8 mV. SEM results indicated that the obtained AgNPs were spherical in shape. Antibacterial activity using dilution method revealed that the minimum inhibitory and minimum bactericidal concentrations of the obtained AgNPs against Streptococcus mutans were 0.025 and 0.1 mg/mL, respectively. Cytotoxicity test of AgNPs on adenocarcinomic human alveolar basal epithelial cells (A549) indicated that the particles impacted against A549 cells. The percentage of cell growth inhibition was 87.5 ± 3.6 % when only 0.1 mg/mL AgNPs was used. These results suggest that ME is the potential reducing agent for green synthesis of AgNPs.

Keywords: antibacterial activity, Moringa oleifera extract, reducing agent, silver nanoparticles

Procedia PDF Downloads 98
1708 Investigation of the Technological Demonstrator 14x B in Different Angle of Attack in Hypersonic Velocity

Authors: Victor Alves Barros Galvão, Israel Da Silveira Rego, Antonio Carlos Oliveira, Paulo Gilberto De Paula Toro

Abstract:

The Brazilian hypersonic aerospace vehicle 14-X B, VHA 14-X B, is a vehicle integrated with the hypersonic airbreathing propulsion system based on supersonic combustion (scramjet), developing in Aerothermodynamics and hypersonic Prof. Henry T. Nagamatsu Laboratory, to conduct demonstration in atmospheric flight at the speed corresponding to Mach number 7 at an altitude of 30km. In the experimental procedure the hypersonic shock tunnel T3 was used, installed in that laboratory. This device simulates the flow over a model is fixed in the test section and can also simulate different atmospheric conditions. The scramjet technology offers substantial advantages to improve aerospace vehicle performance which flies at a hypersonic speed through the Earth's atmosphere by reducing fuel consumption on board. Basically, the scramjet is an aspirated aircraft engine fully integrated that uses oblique/conic shock waves generated during hypersonic flight, to promote the deceleration and compression of atmospheric air in scramjet inlet. During the hypersonic flight, the vehicle VHA 14-X will suffer atmospheric influences, promoting changes in the vehicle's angles of attack (angle that the mean line of vehicle makes with respect to the direction of the flow). Based on this information, a study is conducted to analyze the influences of changes in the vehicle's angle of attack during the atmospheric flight. Analytical theoretical analysis, simulation computational fluid dynamics and experimental investigation are the methodologies used to design a technological demonstrator prior to the flight in the atmosphere. This paper considers analysis of the thermodynamic properties (pressure, temperature, density, sound velocity) in lower surface of the VHA 14-X B. Also, it considers air as an ideal gas and chemical equilibrium, with and without boundary layer, considering changes in the vehicle's angle of attack (positive and negative in relation to the flow) and bi-dimensional expansion wave theory at the expansion section (Theory of Prandtl-Meyer).

Keywords: angle of attack, experimental hypersonic, hypersonic airbreathing propulsion, Scramjet

Procedia PDF Downloads 392
1707 Knee Pain Reduction: Holistic vs. Traditional

Authors: Renee Moten

Abstract:

Introduction: Knee pain becomes chronic because the therapy used focuses only on the symptoms of knee pain and not the causes of knee pain. Preventing knee injuries is not in the toolbox of the traditional practitioner. This research was done to show that we must reduce the inflammation (holistically), reduce the swelling and regain flexibility before considering any type of exercise. This method of performing the correct exercise stops the bowing of the knee, corrects the walking gait, and starts to relieve knee, hip, back, and shoulder pain. Method: The holistic method that is used to heal knees is called the Knee Pain Recipe. It’s a six step system that only uses alternative medicine methods to reduce, relieve and restore knee joint mobility. The system is low cost, with no hospital bills, no physical therapy, and no painkillers that can cause damage to the kidneys and liver. This method has been tested on 200 women with knee, back, hip, and shoulder pain. Results: All 200 women reduce their knee pain by 50%, some by as much as 90%. Learning about ankle and foot flexibility, along with understanding the kinetic chain, helps improve the walking gait, which takes the pressure off the knee, hip and back. The knee pain recipe also has helped to reduce the need for a cortisone injection, stem cell procedures, to take painkillers, and surgeries. What has also been noted in the research was that if the women's knees were too far gone, the Knee Pain Recipe helped prepare the women for knee replacement surgery. Conclusion: It is believed that the Knee Pain Recipe, when performed by men and women from around the world, will give them a holistic alternative to drugs, injections, and surgeries.

Keywords: knee, surgery, healing, holistic

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1706 A Selective and Fast Hydrogen Sensor Using Doped-LaCrO₃ as Sensing Electrode

Authors: He Zhang, Jianxin Yi

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As a clean energy, hydrogen shows many advantages such as renewability, high heat value, and extensive sources and may play an important role in the future society. However, hydrogen is a combustible gas because of its low ignition energy (0.02mJ) and wide explosive limit (4% ~ 74% in air). It is very likely to cause fire hazard or explosion once leakage is happened and not detected in time. Mixed-potential type sensor has attracted much attention in monitoring and detecting hydrogen due to its high response, simple support electronics and long-term stability. Typically, this kind of sensor is consisted of a sensing electrode (SE), a reference electrode (RE) and a solid electrolyte. The SE and RE materials usually display different electrocatalytic abilities to hydrogen. So hydrogen could be detected by measuring the EMF change between the two electrodes. Previous reports indicate that a high-performance sensing electrode is important for improving the sensing characteristics of the sensor. In this report, a planar type mixed-potential hydrogen sensor using La₀.₈Sr₀.₂Cr₀.₅Mn₀.₅O₃₋δ (LSCM) as SE, Pt as RE and yttria-stabilized zirconia (YSZ) as solid electrolyte was developed. The reason for selecting LSCM as sensing electrode is that it shows the high electrocatalytic ability to hydrogen in solid oxide fuel cells. The sensing performance of the fabricated LSCM/YSZ/Pt sensor was tested systemically. The experimental results show that the sensor displays high response to hydrogen. The response values for 100ppm and 1000ppm hydrogen at 450 ºC are -70 mV and -118 mV, respectively. The response time is an important parameter to evaluate a sensor. In this report, the sensor response time decreases with increasing hydrogen concentration and get saturated above 500ppm. The steady response time at 450 ºC is as short as 4s, indicating the sensor shows great potential in practical application to monitor hydrogen. An excellent response repeatability to 100ppm hydrogen at 450 ˚C and a good sensor reproducibility among three sensors were also observed. Meanwhile, the sensor exhibits excellent selectivity to hydrogen compared with several interfering gases such as NO₂, CH₄, CO, C₃H₈ and NH₃. Polarization curves were tested to investigate the sensing mechanism and the results indicated the sensor abide by the mixed-potential mechanism.

Keywords: fire hazard, H₂ sensor, mixed-potential, perovskite

Procedia PDF Downloads 176
1705 Effect of Particle Size and Concentration of Pomegranate (Punica granatum l.) Peel Powder on Suppression of Oxidation of Edible Plant Oils

Authors: D. G. D. C. L. Munasinghe, M. S. Gunawardana, P. H. P. Prasanna, C. S. Ranadheera, T. Madhujith

Abstract:

Lipid oxidation is an important process that affects the shelf life of edible oils. Oxidation produces off flavors, off odors and chemical compounds that lead to adverse health effects. Chemical mechanisms such as autoxidation, photo-oxidation and thermal oxidation are responsible for lipid oxidation. Refined, Bleached and Deodorized (RBD) coconut oil, Virgin Coconut Oil (VCO) and corn oil are widely used plant oils. Pomegranate fruit is known to possess high antioxidative efficacy. Peel of pomegranate contains high antioxidant activity than aril and pulp membrane. The study attempted to study the effect of particle size and concentration of pomegranate peel powder on suppression of oxidation of RBD coconut oil, VCO and corn oil. Pomegranate peel powder was incorporated into each oil sample as micro (< 250 µm) and nano particles (280 - 300 nm) at 100 ppm and 200 ppm concentrations. The control sample of each oil was prepared, devoid of pomegranate peel powder. The stability of oils against autoxidation was evaluated by storing oil samples at 60 °C for 28 days. The level of oxidation was assessed by peroxide value and thiobarbituric acid reactive substances on 0,1,3,5,7,14 and 28 day, respectively. VCO containing pomegranate particles of 280 - 300 nm at 200 ppm showed the highest oxidative stability followed by RBD coconut oil and corn oil. Results revealed that pomegranate peel powder with 280 - 300 nm particle size at 200 ppm concentration was the best in mitigating oxidation of RBD coconut oil, VCO and corn oil. There is a huge potential of utilizing pomegranate peel powder as an antioxidant agent in reducing oxidation of edible plant oils.

Keywords: antioxidant, autoxidation, micro particles, nano particles, pomegranate peel powder

Procedia PDF Downloads 441
1704 Use of Magnetically Separable Molecular Imprinted Polymers for Determination of Pesticides in Food Samples

Authors: Sabir Khan, Sajjad Hussain, Ademar Wong, Maria Del Pilar Taboada Sotomayor

Abstract:

The present work aims to develop magnetic molecularly imprinted polymers (MMIPs) for determination of a selected pesticide (ametryne) using high-performance liquid chromatography (HPLC). Computational simulation can assist the choice of the most suitable monomer for the synthesis of polymers. The (MMIPs) were polymerized at the surface of Fe3O4@SiO2 magnetic nanoparticles (MNPs) using 2-vinylpyradine as functional monomer, ethylene-glycol-dimethacrylate (EGDMA) is a cross-linking agent and 2,2-Azobisisobutyronitrile (AIBN) used as radical initiator. Magnetic non-molecularly imprinted polymer (MNIPs) was also prepared under the same conditions without analyte. The MMIPs were characterized by scanning electron microscopy (SEM), Brunauer, Emmett and Teller (BET) and Fourier transform infrared spectroscopy (FTIR). Pseudo first-order and pseudo second order model were applied to study kinetics of adsorption and it was found that adsorption process followed the pseudo-first-order kinetic model. Adsorption equilibrium data was fitted to Freundlich and Langmuir isotherms and the sorption equilibrium process was well described by Langmuir isotherm mode. The selectivity coefficients (α) of MMIPs for ametryne with respect to atrazine, ciprofloxacin and folic acid were 4.28, 12.32 and 14.53 respectively. The spiked recoveries ranged between 91.33 and 106.80% were obtained. The results showed high affinity and selectivity of MMIPs for pesticide ametryne in the food samples.

Keywords: molecularly imprinted polymer, pesticides, magnetic nanoparticles, adsorption

Procedia PDF Downloads 455
1703 Chemical Analysis, Antioxidant Activity and Antimicrobial Activity of Isolated Compounds and Essential Oil from Callistemon citrinus Leaf

Authors: Manal M. Hamed, Mosad A. Ghareeb, Abdel-Aleem H. Abdel-Aleem, Amal M. Saad, Mohamed S. Abdel-Aziz, Asmaa H. Hadad

Abstract:

Natural products derived from medicinal plants provide unlimited opportunities for a new medication leads because of the unmatched accessibility of chemical variation. Six compounds were isolated from the n-butanol extract of Callistemon citrinus (Family Myrtaceae), they were identified as; nepetolide (1), callislignan A (2), 6,8-dimethoxy-4,5-dimethyl-3-methyleneisochroman-1-one (3), 3-methyl-7-O-benzoyl-β-D-glucopyranoside (4), 5, 7, 3', 5'-tetrahydroxy-6, 8-di-C-methyl flavanone (5), and (2R,3R,4S,5S)-2,4-bis(4-hydroxyphenyl)-3,5-dihydroxy-tetrahydropyran (6). The isolated compounds were evaluated as antioxidant and antimicrobial agents. The antioxidant activities of the compounds were determined using DPPH-radical scavenging and total antioxidant capacity (TAC) assays. The results indicated that compound (5) was most active in its capacity to scavenge free radicals in the DPPH assay [SC50 value, 4.65 ± 0.74μg/mL] compared to the standard ascorbic acid and exhibited the highest activity in the TAC assay (610.45 ± 1.67mg AAE/g compound). The pure isolates were tested for their antimicrobial activity against four pathogenic microbial strains including Staphylococcus aureus, Methicillin-resistant Staphylococcus aureus (MRSA), Pseudomonas aeruginosa and Candida albicans. Also, the GC/MS analysis of its leaves essential oil presented nine identified compounds representing 91% of the total oil constituents. The outcomes got from this study give a reasonable justification for the medicinal uses of Callistemon citrinus plant.

Keywords: Callistemon citrinus, flavanone, antioxidant activity, antimicrobial activity, essential oil, Myrtaceae

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1702 Comparative Study of the Effects of Process Parameters on the Yield of Oil from Melon Seed (Cococynthis citrullus) and Coconut Fruit (Cocos nucifera)

Authors: Ndidi F. Amulu, Patrick E. Amulu, Gordian O. Mbah, Callistus N. Ude

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Comparative analysis of the properties of melon seed, coconut fruit and their oil yield were evaluated in this work using standard analytical technique AOAC. The results of the analysis carried out revealed that the moisture contents of the samples studied are 11.15% (melon) and 7.59% (coconut). The crude lipid content are 46.10% (melon) and 55.15% (coconut).The treatment combinations used (leaching time, leaching temperature and solute: solvent ratio) showed significant difference (p < 0.05) in yield between the samples, with melon oil seed flour having a higher percentage range of oil yield (41.30 – 52.90%) and coconut (36.25 – 49.83%). The physical characterization of the extracted oil was also carried out. The values gotten for refractive index are 1.487 (melon seed oil) and 1.361 (coconut oil) and viscosities are 0.008 (melon seed oil) and 0.002 (coconut oil). The chemical analysis of the extracted oils shows acid value of 1.00mg NaOH/g oil (melon oil), 10.050mg NaOH/g oil (coconut oil) and saponification value of 187.00mg/KOH (melon oil) and 183.26mg/KOH (coconut oil). The iodine value of the melon oil gave 75.00mg I2/g and 81.00mg I2/g for coconut oil. A standard statistical package Minitab version 16.0 was used in the regression analysis and analysis of variance (ANOVA). The statistical software mentioned above was also used to optimize the leaching process. Both samples gave high oil yield at the same optimal conditions. The optimal conditions to obtain highest oil yield ≥ 52% (melon seed) and ≥ 48% (coconut seed) are solute - solvent ratio of 40g/ml, leaching time of 2hours and leaching temperature of 50oC. The two samples studied have potential of yielding oil with melon seed giving the higher yield.

Keywords: Coconut, Melon, Optimization, Processing

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1701 Production of Nitric Oxide by Thienopyrimidine TP053

Authors: Elena G. Salina, Laurent R. Chiarelli, Maria R. Pasca, Vadim A. Makarov

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Tuberculosis is one of the most challenging threats to human health, confronted by the problem of drug resistance. Evidently, new drugs for tuberculosis are urgently needed. Thienopyrimidine TP053 is one of the most promising new antitubercular prodrugs. Mycothiol-dependent reductase Mrx2, encoded by rv2466c, is known to be a TP053 activator; however, the precise mode of action of this compound remained unclear. Being highly active against both replicating and non-replicating tuberculosis bacilli, TP053 also revealed dose-escalating activity for M. tuberculosis-infected murine macrophages. The chemical structure of TP053 is characterized by the presence of NO₂ group which was suggested to be responsible for the toxic effects of the activated compound. Reduction of a nitroaromatic moiety of TP53 by Mrx2 was hypothesized to result in NO release. Analysis of the products of enzymatic activation of TP053 by Mrx2 by the Greiss reagent clearly demonstrated production of nitric oxide in a time-dependent manner. Mass-spectra of cell lysates of TP-treated M. tuberculosis bacilli demonstrated the transformation of TP053 to its non-active metabolite with Mw=261 that corresponds NO release. The mechanism of NO toxicity for bacteria includes DNA damage and degradation of iron-sulfur centers, especially under oxygen depletion. Thus, TP-053 drug-like scaffold is prospective for further development of novel anti-TB drug. This work was financially supported by the Russian Foundation for Basic Research (Grant 17-04-00342).

Keywords: drug discovery, M. tuberculosis, nitric oxide, NO donors

Procedia PDF Downloads 136
1700 Design of Liquid Crystal Based Interface to Study the Interaction of Gram Negative Bacterial Endotoxin with Milk Protein Lactoferrin

Authors: Dibyendu Das, Santanu Kumar Pal

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Milk protein lactoferrin (Lf) exhibits potent antibacterial activity due to its interaction with Gram-negative bacterial cell membrane component, lipopolysaccharide (LPS). This paper represents fabrication of new Liquid crystals (LCs) based biosensors to explore the interaction between Lf and LPS. LPS self-assembled at aqueous/LCs interface and orients interfacial nematic 4-cyano-4’- pentylbiphenyl (5CB) LCs in a homeotropic fashion (exhibiting dark optical image under polarized optical microscope). Interestingly, on the exposure of Lf on LPS decorated aqueous/LCs interface, an optical image of LCs changed from dark to bright indicating an ordering alteration of interfacial LCs from homeotropic to tilted/planar state. The ordering transition reflects strong binding between Lf and interfacial LPS that, in turn, perturbs the orientation of LCs. With the help of epifluorescence microscopy, we further affirmed the interfacial LPS-Lf binding event by imaging the presence of FITC tagged Lf at the LPS laden aqueous/LCs interface. Finally, we have investigated the conformational behavior of Lf in solution as well as in the presence of LPS using Circular Dichroism (CD) spectroscopy and further reconfirmed with Vibrational Circular Dichroism (VCD) spectroscopy where we found that Lf undergoes alpha-helix to random coil-like structure in the presence of LPS. As a whole the entire results described in this paper establish a robust approach to envisage the interaction between LPS and Lf through the ordering transitions of LCs at aqueous/LCs interface.

Keywords: endotoxin, interface, lactoferrin, lipopolysaccharide

Procedia PDF Downloads 253