Search results for: in vitro drug release

Authors: Cleto J. Sauer Jr., Rita C. Sauer, Chaider G. Andrade, Doris F. Rabelo

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Introduction: Endotracheal Intubation (ETI) is a procedure for clinical management of patients with severe clinical presentation of COVID-19 disease. Realistic simulation (RS) is an active learning methodology utilized for clinical skill's improvement. To improve ETI skills of public health network's physicians from Recôncavo da Bahia region in Brazil, during COVID-19 outbreak, RS training was planned and carried out. Training scenario included the Nasco Lifeform realistic simulator, and three actions were simulated: ETI procedure, sedative drugs management, and bougie guide utilization. Training intervention occurred between May and June 2020, as an interinstitutional cooperation between the Health's Department of Bahia State and the Federal University from Recôncavo da Bahia. Objective: The main objective is to report the effects on participants' self-confidence perception for ETI procedure after RS based training. Methods: This is a descriptive study, with secondary data extracted from questionnaires applied throughout RS training. Priority workplace, time from last intubation, and knowledge about bougie were reported on a preparticipation questionnaire. Additionally, participants completed pre- and post-training qualitative self-assessment (10-point Likert scale) regarding self-confidence perception in performing each of simulated actions. Distribution analysis for qualitative data was performed with Wilcoxon Signed Rank Test, and self-confidence increase analysis in frequency contingency tables with Fisher's Exact Test. Results: 36 physicians participated of training, 25 (69%) from primary care setting, 25 (69%) performed ETI over a year ago, and only 4 (11%) had previous knowledge about the bougie guide utilization. There was an increase in self-confidence medians for all three simulated actions. Medians (variation) for self-confidence before and after training, for each simulated action were as follows: ETI [5 (1-9) vs. 8 (6-10) (p < 0.0001)]; Sedative drug management [5 (1-9) vs. 8 (4-10) (p < 0.0001)]; Bougie guide utilization [2.5 (1-7) vs. 8 (4-10) (p < 0.0001)]. Among those who performed ETI over a year ago (n = 25), an increase in self-confidence greater than 3 points for ETI was reported by 23 vs. 2 physicians (p = 0.0002), and by 21 vs. 4 (p = 0.03) for sedative drugs management. Conclusions: RS training contributed to self-confidence increase in performing ETI. Among participants who performed ETI over a year, there was a significant association between RS training and increase of more than 3 points in self-confidence, both for ETI and sedative drug management. Training with RS methodology is suitable for ETI confidence enhancement during COVID-19 outbreak.

Keywords: confidence, COVID-19, endotracheal intubation, realistic simulation

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Authors: F. Madani, M. Doudi, L. Rahimzadeh Torabi

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The irregular consumption of current antibiotics contributes to an escalation in antibiotic resistance among urinary pathogens on a global scale. The objective of this research was to investigate the process of biologically synthesized silver nanoparticles through the utilization of Zataria multiflora extract. Additionally, the study aimed to evaluate the efficacy of these synthesized nanoparticles in inhibiting the growth of multi-drug resistant negative bacillus bacteria, which commonly contribute to urinary tract infections. The botanical specimen utilized in the current research investigation was Z. multiflora, and its extract was produced employing the Soxhlet extraction technique. The study examined the green synthesis conditions of silver nanoparticles by considering three key parameters: the quantity of extract used, the concentration of silver nitrate salt, and the temperature. The particle dimensions were ascertained using the Zetasizer technique. In order to identify synthesized Silver nanoparticles TEM, XRD, and FTIR methods were used. For evaluating the antibacterial effects of nanoparticles synthesized through a biological method, different concentrations of silver nanoparticles were studied on 140 cases of Multiple drug resistance (MDR) bacteria strains Escherichia coli, Klebsiella pneumoniae, Enterobacter aerogenes, Proteus vulgaris,Citrobacter freundii, Acinetobacter bumanii and Pseudomonas aeruginosa, (each genus of bacteria, 20 samples), which all were MDR and cause urinary tract infections, for identification of bacteria were used of PCR test and laboratory methods (Agar well diffusion and Microdilution methods) to assess their sensitivity to Nanoparticles. The data were subjected to analysis using the statistical software SPSS, specifically employing nonparametric Kruskal-Wallis and Mann-Whitney tests. This study yielded noteworthy findings regarding the impacts of varying concentrations of silver nitrate, different quantities of Z. multiflora extract, and levels of temperature on nanoparticles. Specifically, it was observed that an increase in the concentration of silver nitrate, extract amount, and temperature resulted in a reduction in the size of the nanoparticles synthesized. However, the impact of the aforementioned factors on the index of particle diffusion was found to be statistically non-significant. According to the transmission electron microscopy (TEM) findings, the particles exhibited predominantly spherical morphology, with a diameter spanning from 25 to 50 nanometers. Nanoparticles in the examined sample. Nanocrystals of silver. FTIR method illustrated that the spectrums of Z. multiflora and synthesized nanoparticles had clear peaks in the ranges of 1500-2000, and 3500 - 4000. The obtained results of antibacterial effects of different concentrations of silver nanoparticles on according to agar well diffusion and microdilution method, biologically synthesized nanoparticles showed 1000 mg /ml highest and lowest mean inhibition zone diameter in E. coli, A. bumanii 23 and 15mm, respectively. MIC was observed for all of bacteria 125 mg/ml and for A. bumanii 250 mg/ml. Comparing the growth inhibitory effect of chemically synthesized the results obtained from the experiment indicated that both nanoparticles and biologically synthesized nanoparticles exhibit a notable growth inhibition effect. Specifically, the chemical method of synthesizing nanoparticles demonstrated the highest level of growth inhibition at a concentration of 62.5 mg/mL The present study demonstrated an inhibitory effect on bacterial growth, facilitating the causative factors of urine infection and multidrug resistance (MDR).

Keywords: multiple drug resistance, negative bacillus bacteria, urine infection, Zataria multiflora

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Authors: Supriya Majumder, Pabitra Banik

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Fates of Arsenic (As) on the soil-plant environment belong to the critical emerging issue, which in turn to appraises the threatening implications of a human health risk — assessing the dynamics of As in soil solid components are likely to impose its potential availability towards plant uptake. In the present context, we introduced an improved Sequential Extraction Procedure (SEP) questioning to identify solid-phase speciation of As in paddy soil under variable soil environmental conditions during two consecutive seasons of rice cultivation practices. We coupled gradients of water management practices with the addition of fertilizer amendments to assess the changes in a partition of As through a field experimental study during monsoon and post-monsoon season using two rice cultivars. Water management regimes were varied based on the methods of cultivation of rice by Conventional (waterlogged) vis-a-vis System of Rice Intensification-SRI (saturated). Fertilizer amendment through the nutrient treatment of absolute control, NPK-RD, NPK-RD + Calcium silicate, NPK-RD + Ferrous sulfate, Farmyard manure (FYM), FYM + Calcium silicate, FYM + Ferrous sulfate, Vermicompost (VC), VC + Calcium silicate, VC + Ferrous sulfate were selected to construct the study. After harvest, soil samples were sequentially extracted to estimate partition of As among the different fractions such as: exchangeable (F1), specifically sorbed (F2), As bound to amorphous Fe oxides (F3), crystalline Fe oxides (F4), organic matter (F5) and residual phase (F6). Results showed that the major proportions of As were found in F3, F4 and F6, whereas F1 exhibited the lowest proportion of total soil As. Among the nutrient treatment mediated changes on As fractions, the application of organic manure and ferrous sulfate were significantly found to restrict the release of As from exchangeable phase. Meanwhile, conventional practice produced much higher release of As from F1 as compared to SRI, which may substantially increase the environmental risk. In contrast, SRI practice was found to retain a significantly higher proportion of As in F2, F3, and F4 phase resulting restricted mobilization of As. This was critically reflected towards rice grain As bioavailability where the reduction in grain As concentration of 33% and 55% in SRI concerning conventional treatment (p <0.05) during monsoon and post-monsoon season respectively. Also, prediction assay for rice grain As bioavailability based on the linear regression model was performed. Results demonstrated that rice grain As concentration was positively correlated with As concentration in F1 and negatively correlated with F2, F3, and F4 with a satisfactory level of variation being explained (p <0.001). Finally, we conclude that F1, F2, F3 and F4 are the major soil. As fractions critically may govern the potential availability of As in soil and suggest that rice cultivation with the SRI treatment is particularly at less risk of As availability in soil. Such exhaustive information may be useful for adopting certain management practices for rice grown in contaminated soil concerning to the environmental issues in particular.

Keywords: arsenic, fractionation, paddy soil, potential availability

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Authors: Van Tran Thi Thuy, Dukjoon Kim

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A series of pH- and thermosensitive poly(N-isopropyl acrylamide-co-acrylic acid) were synthesized by radical polymerization and grafted on poly succinimide backbones. The poly succinimide derivatives synthesized were coated on iron oxide magnetic nanoparticles for potential applications in drug delivery systems with theranostic and molecular imaging. The structure of polymer shell was confirmed by FT-IR, H-NMR spectroscopies. Its thermal behavior was tested by UV-Vis spectroscopy. The particle size and its distribution are measured by dynamic light scattering (DLS) and transmission electron microscope (TEM). The mean diameter of the core-shell structure is from 20 to 80 nm.

Keywords: magnetic, nano, PNIPAM, polysuccinimide

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Authors: Yazan S. Khaled, Shazana Shamsuddin, Jim Tiernan, Mike McPherson, Thomas Hughes, Paul Millner, David G. Jayne

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Introduction: There is a need for real-time imaging of colorectal cancer (CRC) to allow tailored surgery to the disease stage. Fluorescence guided laparoscopic imaging of primary colorectal cancer and the draining lymphatics would potentially bring stratified surgery into clinical practice and realign future CRC management to the needs of patients. Fluorescent nanoparticles can offer many advantages in terms of intra-operative imaging and therapy (theranostic) in comparison with traditional soluble reagents. Nanoparticles can be functionalised with diverse reagents and then targeted to the correct tissue using an antibody or Affimer (artificial binding protein). We aimed to develop and test fluorescent silica nanoparticles and targeted against CRC using an anti-carcinoembryonic antigen (CEA) Affimer (Aff). Methods: Anti-CEA and control Myoglobin Affimer binders were subcloned into the expressing vector pET11 followed by transformation into BL21 Star™ (DE3) E.coli. The expression of Affimer binders was induced using 0.1 mM isopropyl β-D-1-thiogalactopyranoside (IPTG). Cells were harvested, lysed and purified using nickle chelating affinity chromatography. The photosensitiser Foslip (soluble analogue of 5,10,15,20-Tetra(m-hydroxyphenyl) chlorin) was incorporated into the core of silica nanoparticles using water-in-oil microemulsion technique. Anti-CEA or control Affs were conjugated to silica nanoparticles surface using sulfosuccinimidyl-4-(N-maleimidomethyl) cyclohexane-1-carboxylate (sulfo SMCC) chemical linker. Binding of CEA-Aff or control nanoparticles to colorectal cancer cells (LoVo, LS174T and HC116) was quantified in vitro using confocal microscopy. Results: The molecular weights of the obtained band of Affimers were ~12.5KDa while the diameter of functionalised silica nanoparticles was ~80nm. CEA-Affimer targeted nanoparticles demonstrated 9.4, 5.8 and 2.5 fold greater fluorescence than control in, LoVo, LS174T and HCT116 cells respectively (p < 0.002) for the single slice analysis. A similar pattern of successful CEA-targeted fluorescence was observed in the maximum image projection analysis, with CEA-targeted nanoparticles demonstrating 4.1, 2.9 and 2.4 fold greater fluorescence than control particles in LoVo, LS174T, and HCT116 cells respectively (p < 0.0002). There was no significant difference in fluorescence for CEA-Affimer vs. CEA-Antibody targeted nanoparticles. Conclusion: We are the first to demonstrate that Foslip-doped silica nanoparticles conjugated to anti-CEA Affimers via SMCC allowed tumour cell-specific fluorescent targeting in vitro, and had shown sufficient promise to justify testing in an animal model of colorectal cancer. CEA-Affimer appears to be a suitable targeting molecule to replace CEA-Antibody. Targeted silica nanoparticles loaded with Foslip photosensitiser is now being optimised to drive photodynamic killing, via reactive oxygen generation.

Keywords: colorectal cancer, silica nanoparticles, Affimers, antibodies, imaging

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Authors: Fikri Suwaileh

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In the reverse osmosis (RO) water treatment plant, operation was suffering from several leaks on the acid injection point spool and downstream spools, due to insufficient injection monitoring and the coating failure leading to pin holes. The paper will go over the background of the leaks in the acid injection point, the process in the RO plant, the material, and coating used in the existing spools, the impact of these repeated leaks, the type of damage mechanism that occurred in the system due to the manner of acid injection and the heat in the spools, which lead to coating failure, leaks and water release. This paper will also look at the analysis, both the short- and long-term recommendations, and the utilization of Teflon internal lining to stop the leaks. Sharing this case study will enhance the knowledge of the importance of taking all factors that will lead to leaks in the acid injection points, along with the importance of utilizing the appropriate coating material lining to enhance the full system.

Keywords: corrosion, coating, raw water, lining

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Authors: Abdulrahman Sumayli

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Natural Zinc has many significant biological functions, including developments and sustainable of bones and wound healing. Metallic zinc has recently been explored as potential biomaterials that have preferable biodegradable, biocompatible, and mechanical properties. Pure metal zinc has a preferable physical and mechanical properties for biodegradable and biocompatible applications such as density and modulus of elasticity. The aim of the research is to make different Zn-based metallic alloys and test them effectively to be used as biocompatible and biodegradable materials in the field biomedical application. Microstructure study of the as-cast alloys will be examined using SEM (scanning electron microscope) followed by X-ray diffraction investigated so as to evaluate phase constitution of the designed alloys. After that, immersion test and electrochemical test will be applied to the designed alloys so as to study bio corrosion behaviour of the proposed alloys. Finally, in vitro cytocompatibility well conducted to study biocompatibility of the made alloys.

Keywords: Zn-based alloys, biodegradable and biocompatible materials, cytotoxicity test, neutron synchrotron imaging

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Authors: Amrei Voelkner, Nils Peters, Thomas Mannheim

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The worldwide exponential growth of the population and the simultaneous increasing food production requires the strategic realization of sustainable and improved cultivation systems to ensure the fertility of arable land and to guarantee the food supply for the whole world. To fulfill this target, large quantities of fertilizers have to be applied to the field, but the long-term environmental impacts remain uncertain. Thus, a combined system would be necessary to increase the nutrient availability for plants while reducing nutrient losses (e.g. NO3- by leaching) to the environment. To enhance the nutrient efficiency, polymer coated fertilizer with a controlled release behavior have been developed. This kind of fertilizer ensures a delayed release of nutrients to synchronize the nutrient supply with the demand of different crops. In the last decades, research focused primarily on semi-permeable polyurethane coatings, which remain in the soil for a long period after the complete solvation of the fertilizer core. Within the implementation of the new European Regulation Directive the replacement of non-degradable synthetic polymers by degradable coatings is necessary. It was, therefore, the objective of this study to develop a total biodegradable polymer (to CO2 and H2O) coating according to ISO 17556 and to compare the retarding effect of the biodegradable coatings with commercially available non-degradable products. To investigate the effect of ten selected coated urea fertilizer on the yield of annual ryegrass and maize, the fresh and dry mass, the percentage of total nitrogen and main nutrients were analyzed in greenhouse experiments in sixfold replications using near-infrared spectroscopy. For the experiments, a homogenized and air-dried loamy sand (Cambic Luvisol) was equipped with a basic fertilization of P, K, Mg and S. To investigate the effect of nitrogen level increase, three levels (80%, 100%, 120%) were established, whereas the impact of CRF granules was determined using a N-level of 100%. Additionally, leaching of NO3- from pots planted with annual ryegrass was examined to evaluate the retention capacity of urea by the polymer coating. For this, leachate from Kick-Brauckmann-Pots was collected daily and analyzed for total nitrogen, NO3- and NH4+ in twofold repetition once a week using near-infrared spectroscopy. We summarize from the results that the coated fertilizer have a clear impact on the yield of annual ryegrass and maize. Compared to the control, an increase of fresh and dry mass could be recognized. Partially, the non-degradable coatings showed a retarding effect for a longer period, which was however reflected by a lower fresh and dry mass. It was ascertained that the percentage of leached-out nitrate could be reduced markedly. As a conclusion, it could be pointed out that the impact of coated fertilizer of all polymer types might contribute to a reduction of negative environmental impacts in addition to their fertilizing effect.

Keywords: biodegradable polymers, coating, enhanced efficiency fertilizers, nitrate leaching

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Authors: Shahriar Shahbazpanahi, Mohammad Hemen Jannaty, Alaleh Kamgar

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Shear strengthening can be carried out in concrete structures by external fibre reinforced polymer (FRP). In the present investigation, a new fracture mechanics model is developed to model side face of strengthened concrete beam by external FRP. Discrete crack is simulated by a spring element with softening behavior ahead of the crack tip to model the cohesive zone in concrete. A truss element is used, parallel to the spring element, to simulate the energy dissipation rate by the FRP. The strain energy release rate is calculated directly by using a virtual crack closure technique and then, the crack propagation criterion is presented. The results are found acceptable when compared to previous experimental results and ABAQUS software data. It is observed that the length of the fracture process zone (FPZ) increases with the application of FRP in side face at the same load in comparison with that of the control beam.

Keywords: FPZ, fracture, FRP, shear

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Authors: Yung-Chih Kuo, Che-Yu Lin, Jay-Shake Li, Yung-I Lou

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Curcumin (CRM) and nerve growth factor (NGF) were entrapped in liposomes (LIP) with cardiolipin (CL) to downregulate the phosphorylation of mitogen-activated protein kinases for Alzheimer’s disease (AD) management. AD belongs to neurodegenerative disorder with a gradual loss of memory, yielding irreversible dementia. CL-conjugated LIP loaded with CRM (CRM-CL/LIP) and that with NGF (NGF-CL/LIP) were applied to AD models of SK-N-MC cells and Wistar rats with an insult of β-amyloid peptide (Aβ). Lipids comprising 1,2-dipalmitoyl-sn-glycero-3- phosphocholine (Avanti Polar Lipids, Alabaster, AL), 1',3'-bis[1,2- dimyristoyl-sn-glycero-3-phospho]-sn-glycerol (CL; Avanti Polar Lipids), 1,2-dipalmitoyl-sn-glycero-3-phosphoethanolamine-N- [methoxy(polyethylene glycol)-2000] (Avanti Polar Lipids), 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[carboxy(polyethylene glycol)-2000] (Avanti Polar Lipids) and CRM (Sigma–Aldrich, St. Louis, MO) were dissolved in chloroform (J. T. Baker, Phillipsburg, NJ) and condensed using a rotary evaporator (Panchum, Kaohsiung, Taiwan). Human β-NGF (Alomone Lab, Jerusalem, Israel) was added in the aqueous phase. Wheat germ agglutinin (WGA; Medicago AB, Uppsala, Sweden) was grafted on LIP loaded with CRM for (WGA-CRM-LIP) and CL-conjugated LIP loaded with CRM (WGA-CRM-CL/LIP) using 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide (Sigma–Aldrich) and N-hydroxysuccinimide (Alfa Aesar, Ward Hill, MA). The protein samples of SK-N-MC cells (American Type Tissue Collection, Rockville, MD) were used for sodium dodecyl sulfate (Sigma–Aldrich) polyacrylamide gel (Sigma–Aldrich) electrophoresis. In animal study, the LIP formulations were administered by intravenous injection via a tail vein of male Wistar rats (250–280 g, 8 weeks, BioLasco, Taipei, Taiwan), which were housed in the Animal Laboratory of National Chung Cheng University in accordance with the institutional guidelines and the guidelines of Animal Protection Committee under the Council of Agriculture of the Republic of China. We found that CRM-CL/LIP could inhibit the expressions of phosphorylated p38 (p-p38), p-Jun N-terminal kinase (p-JNK), and p-tau protein at serine 202 (p-Ser202) to retard the neuronal apoptosis. Free CRM and released CRM from CRM-LIP and CRM-CL/LIP were not in a straightforward manner to effectively inhibit the expression of p-p38 and p-JNK in the cytoplasm. In addition, NGF-CL/LIP enhanced the quantities of p-neurotrophic tyrosine kinase receptor type 1 (p-TrkA) and p-extracellular-signal-regulated kinase 5 (p-ERK5), preventing the Aβ-induced degeneration of neurons. The membrane fusion of NGF-LIP activated the ERK5 pathway and the targeting capacity of NGF-CL/LIP enhanced the possibility of released NGF to affect the TrkA level. Moreover, WGA-CRM-LIP improved the permeation of CRM across the blood–brain barrier (BBB) and significantly reduced the Aβ plaque deposition and malondialdehyde level and increased the percentage of normal neurons and cholinergic function in the hippocampus of AD rats. This was mainly because the encapsulated CRM was protected by LIP against a rapid degradation in the blood. Furthermore, WGA on LIP could target N-acetylglucosamine on endothelia and increased the quantity of CRM transported across the BBB. In addition, WGA-CRM-CL/LIP could be effective in suppressing the synthesis of acetylcholinesterase and reduced the decomposition of acetylcholine for better neurotransmission. Based on the in vitro and in vivo evidences, WGA-CRM-CL/LIP can rescue neurons from apoptosis in the brain and can be a promising drug delivery system for clinical AD therapy.

Keywords: Alzheimer’s disease, β-amyloid, liposome, mitogen-activated protein kinase

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Authors: Boudjelal Amel

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Arisarum vulgare, a member of the Araceae family, is an herbaceous perennial widely distributed in the Mediterranean region. A. vulgare is recognized for its medicinal properties and holds significant traditional importance in Algeria for the treatment of various human ailments, including pain, infections, inflammation, digestive disorders, skin problems, eczema, cancer, wounds, burns and gynecological diseases. Despite its extensive traditional use, scientific exploration of A. vulgare remains limited. The study aims to investigate for the first time the therapeutic potential of A. vulgare ethanolic extract obtained by ultrasound-assisted extraction. The chemical composition of the extract was determined by LC-MS/MS analysis. For in vitro phytopharmacological evaluation, several assays, including DPPH, ABTS, FRAP and reducing power, were employed to evaluate the antioxidant activity. The antibacterial activity was assessed againt Escherichia coli, Salmonella typhimurium, Staphylococus aureus, Enterococcus feacium by disk diffusion and microdilution methods. The possible inhibitory activity of ethanolic extract was analyzed against the cholinesterases enzymes (AChE and BChE). The DNA protection activity of A. vulgare ethanolic extract was estimated using the agarose gel electrophoresis method. The capacities of the extract to protect plasmid DNA (pBR322) from the oxidizing effects of H2O2 and UV treatment were evaluated by their DNA-breaking forms. The in vivo wound healing potential of a traditional ointment containing 5% of A. vulgare ethanolic extract was also investigated. The LC-MS/MS profiling of the extract revealed the presence of various bioactive compounds, including naringenin, chlorogenic, vanillic, cafeic, coumaric acids, trans-cinnamic and trans ferrulic acids. The plant extract presented considerable antioxidant potential, being the most active for Reducing power (0,07326±0.001 mg/ml) and DPPH (0.14±0.004 mg/ml). The extract showed the highest inhibition zone diameter against Enterococcus feacium (36±0.1 mm). The ethanolic extract of A. vulgare suppressed the growth of Staphylococus aureus, Escherichia coli and Salmonella typhimurium according to the MIC values. The extract of the plant significantly inhibited both AChE and BChE enzymes. DNA protection activity of the A. vulgare extract was determined as 90.41% for form I and 51.92% for form II. The in vivo experiments showed that 5% ethanolic extract ointment accelerated the wound healing process. The topical application of the traditional formulation enhanced wound closure (95,36±0,6 %) and improved histological parameters in the treated group compared to the control groups. The promising biological properties of Arisarum vulgare revealed that the plant could be appraised as a potential origin of bioactive molecules having multifunctional medicinal uses.

Keywords: arisarum vulgare, LC-MS/MS, antioxidant activity, antimicrobial activity, cholinesterases enzymes inhibition, dna-damage activity, in vivo wound healing

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Authors: Fernanda Gonçalves, Karla Alcântara, Vanessa Moura, Patrícia Nolasco, Jorge Kalil, Maristela Hernandez

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Introduction: Atherosclerosis is a chronic disease where two striking features are observed: retention of lipids and inflammation. Understanding the interaction between immune cells and lipoproteins involved in atherogenesis are urgent challenges, since cardiovascular diseases are the leading cause of death worldwide. Macrophages are critical to the development of atherosclerotic plaques and in the perpetuation of inflammation in these lesions. These cells are also directly involved in unstable plaque rupture. Recently different populations of macrophages are being identified in atherosclerotic lesions. Although the presence of M2 macrophages (macrophages activated by the alternative pathway, eg. The IL-4) has been identified, the function of these cells in atherosclerosis is not yet defined. M2 macrophages have a high endocytic capacity, they promote remodeling of tissues and to have anti-inflammatory activity. However, in atherosclerosis, especially unstable plaques, severe inflammatory reaction, accumulation of cellular debris and intense degradation of the tissue is observed. Thus, it is possible that the M2 macrophages have altered function (phenotype) in atherosclerosis. Objective: Our aim is to evaluate if the presence of oxidized LDL alters the phenotype and function of M2 macrophages in vitro. Methods: For this, we will evaluate whether the addition of lipoprotein in M2 macrophages differentiated in vitro with IL -4 induces 1) a reduction in the secretion of anti-inflammatory cytokines (CBA and ELISA), 2) secretion of inflammatory cytokines (CBA and ELISA), 3) expression of cell activation markers (Flow cytometry), 4) alteration in gene expression of molecules adhesion and extracellular matrix (Real-Time PCR) and 5) Matrix degradation (confocal microscopy). Results: In oxLDL stimulated M2 macrophages cultures we did not find any differences in the expression of the cell surface markers tested, including: HLA-DR, CD80, CD86, CD206, CD163 and CD36. Also, cultures stimulated with oxLDL had similar phagocytic capacity when compared to unstimulated cells. However, in the supernatant of these cultures an increase in the secretion of the pro-inflammatory cytokine IL-8 was detected. No significant changes where observed in IL-6, IL-10, IL-12 and IL-1b levels. The culture supernatant also induced massive extracellular matrix (produced by mouse embryo fibroblast) filaments degradation. When evaluating the expression of 84 extracellular matrix and adhesion molecules genes, we observed that the stimulation of oxLDL in M2 macrophages decreased 47% of the genes and increased the expression of only 3% of the genes. In particular we noted that oxLDL inhibit the expression of 60% of the genes constituents of extracellular matrix and collagen expressed by these cells, including fibronectin1 and collagen VI. We also observed a decrease in the expression of matrix protease inhibitors, such as TIMP 2. On the opposite, the matricellular protein thrombospondin had a 12 fold increase in gene expression. In the presence of native LDL 90% of the genes had no altered expression. Conclusion: M2 macrophages stimulated with oxLDL secrete the pro-inflammatory cytokine IL-8, have an altered extracellular matrix constituents gene expression, and promote the degradation of extracellular matrix. M2 macrophages may contribute to the perpetuation of inflammation in atherosclerosis and to plaque rupture.

Keywords: atherosclerosis, LDL, macrophages, m2

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Authors: Tareg Belali, Mosleh Abomughaid, Muhanad Alhujaily

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HNF4a is one of the steroid hormone receptor family of transcription factors with roles in the development of the liver and the regulation of several critical metabolic pathways, such as glycolysis, drug metabolism, and apolipoproteins and blood coagulation. The transcriptional potency of HNF4a is well known due to its involvement in diabetes and other metabolic diseases. However, recently HNF4a has been discovered to be closely associated with several haematological disorders, mainly because of genetic mutations, drugs, and hepatic disorders. We review HNF4a structure and function and its role in haematological disorders. We discuss possible good therapies that are based on targeting HNF4a.

Keywords: hepatocyte nuclear factor 4 alpha, HNF4a nuclear receptor, steroid hormone receptor family of transcription factors, hematological disorders

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Authors: Joe Collins, Matthias Rother

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Background: Oral non-steroidal anti-inflammatory drugs (NSAIDs) are widely used for the relief of joint pain during and post-exercise. However, oral NSAIDs increase the risk of systemic side effects, even in healthy individuals, and retard recovery from muscle soreness. TDT 064 (Flexiseq®), a topical formulation containing ultra-deformable drug-free Sequessome™ vesicles, has demonstrated equivalent efficacy to oral celecoxib in reducing osteoarthritis-associated joint pain and stiffness. TDT 064 does not cause NSAID-related adverse effects. We describe clinical study data and a case report on the effectiveness of TDT 064 in reducing joint pain after exercise. Methods: Participants with a pain score ≥3 (10-point scale) 12–16 hours post-exercise were randomized to receive TDT 064 plus oral placebo, TDT 064 plus oral ketoprofen, or ketoprofen in ultra-deformable phospholipid vesicles plus oral placebo. Results: In the 168 study participants, pain scores were significantly higher with oral ketoprofen plus TDT 064 than with TDT 064 plus placebo in the 7 days post-exercise (P = 0.0240) and recovery from muscle soreness was significantly longer (P = 0.0262). There was a low incidence of adverse events. These data are supported by clinical experience. A 24-year-old male professional rugby player suffered a traumatic lisfranc fracture in March 2014 and underwent operative reconstruction. He had no relevant medical history and was not receiving concomitant medications. He had undergone anterior cruciate ligament reconstruction in 2008. The patient reported restricted training due to pain (score 7/10), stiffness (score 9/10) and poor function, as well as pain when changing direction and running on consecutive days. In July 2014 he started using TDT 064 twice daily at the recommended dose. In November 2014 he noted reduced pain on running (score 2-3/10), decreased morning stiffness (score 4/10) and improved joint mobility and was able to return to competitive rugby without restrictions. No side effects of TDT 064 were reported. Conclusions: TDT 064 shows efficacy against exercise- and injury-induced joint pain, as well as that associated with osteoarthritis. It does not retard muscle soreness recovery after exercise compared with an oral NSAID, making it an alternative approach for the treatment of joint pain during and post-exercise.

Keywords: exercise, joint pain, TDT 064, phospholipid vesicles

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Authors: Magda Mahmoud Amin Sabbour, El-Sayed H. Shaurub

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The Indian meal moth Plodia interpunctella (Hübner) (Lepidoptera: Pyralidae), of stored grain pests which destroy the seed completely. Their larval stages feed on the nutrient germinating kernels part found in the seeds grain. This leads to a reduction causing a badness to seed germination and seed viability. It controlled by many insecticides which pollute and cusses a harmful diseases to human being. Three tested oils were evaluated on this target pests. Plant extracts, essential oils and medical oils are materials which used to control many stored pests. Plant oils extracts have a lower effects on parasites and predators and not pollute the medium. By using the apparatus gas chromatography flame ionization detector gas chromatography–analysis of three essential oil tested. This research was point to explore and appreciation the activity of three oils and nano gel Beauvericin against P. interpunctella in the laboratory conditions and in the store conditions. The three essential oil tested proved that, percentage of α-Pinene recoded 7.76, 7.72 and 6.66 for C. cyminum, A. squamosal and G. officinale respectively. The composition of the β-Pinene recoded 4.61, 8.92 and 30.63 for the corresponding oils tested. Results showed that after analytically the oils tested, the effective compound of C. cyminum oil are p-cyinene and Terpinene. Results obtained show that the LC50 recorded 125, 112, 55 and 20 ppm after P. interpunctella treated with medical oils of Guaiacum officinale, Annona squamosa, Cuminum cyminum and Beauvericin 3% respectively. The accumulative mortality of P. interpunctella after treated with A.squamosa oil-loaded nanogels which showed that it is the highest oils from infestations recoded when the seed treated with 3% after 48 days, the accumulations obtained 44% at followed by 24 after24 days of storage. Results, cleared that the seed protection by G. officinale recorded 40% at concentrations of 3% after 48 days of storage seeds. C. cyminum was the highest mortality by 98, at concentrations 3%. The highest seed protection proved after C. cyminum oil-loaded nanogels 14% followed by G. officinale 29% and A.squamosa 44%.when the seeds treated with Beauvericin 3%. Results of this work cleared that the essential medical oils have a useful action effect on target insects. Plant essential and medical oils, their active ingredient have potentially high bioactivity against on P. interpunctella. The medical and essential oils incorporation and usage the nano-formulation release stopped the highly degradation vaporization and the increasing in the constancy, and save the lower effectiveness of the dosage/application. The research results proved that the highest seed protection obtained after C. cyminum oil-loaded nanogels followed by G. officinale and A.squamosa. It could be complemented that P. interpunctella were more susceptible to medical oils loaded nanogel (MOLNs ) than medical oils only (MO). MOLNs had best lower amount of the residual activity than MO only. MOLNs might mend the insecticidal action of the medical oil tested by the slow effective release of the medical oils to control P. interpunctella mostly at the lower doses.

Keywords: Cuminum cyminum, annona squamosa, guaiacum officinale, beauvericin 3 %, plodia interpunctella

Procedia PDF Downloads 120

Authors: Andrew Gray, Zhibing Zhang

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The ability for consumer products to deliver a sustained perfume response can be a key driver for a variety of applications. Many compounds in perfume oils are highly volatile, meaning they readily evaporate once the product is applied, and the longevity of the scent is poor. Perfume capsules have been introduced as a means of abating this evaporation once the product has been delivered. The impermeable capsules are aimed to be stable within the formulation, and remain intact during delivery to the desired substrate, only rupturing to release the core perfume oil through application of mechanical force applied by the consumer. This opens up the possibility of obtaining an olfactive response hours, weeks or even months after delivery, depending on the nature of the desired application. Tailoring the properties of the polymeric capsules to better address the needs of the application is not a trivial challenge and currently design of capsules is largely done by trial and error. The aim of this work is to have more predictive methods for capsule design depending on the consumer application. This means refining formulations such that they rupture at the right time for the specific consumer application, not too early, not too late. Finding the right balance between these extremes is essential if a benefit is sought with respect to neat addition of perfume to formulations. It is important to understand the forces that influence capsule rupture, first, by quantifying the magnitude of these different forces, and then by assessing bulk rupture in real-world applications to understand how capsules actually respond. Samples were provided by an industrial partner and the mechanical properties of individual capsules within the samples were characterized via a micromanipulation technique, developed by Professor Zhang at the University of Birmingham. The capsules were synthesized such as to change one particular physicochemical property at a time, such as core: wall material ratio, and the average size of capsules. Analysis of shell thickness via Transmission Electron Microscopy, size distribution via the use of a Mastersizer, as well as a variety of other techniques confirmed that only one particular physicochemical property was altered for each sample. The mechanical analysis was subsequently undertaken, showing the effect that changing certain capsule properties had on the response under compression. It was, however, important to link this fundamental mechanical response to capsule performance in real-world applications. As such, the capsule samples were introduced to a formulation and exposed to full scale stresses. GC-MS headspace analysis of the perfume oil released from broken capsules enabled quantification of what the relative strengths of capsules truly means for product performance. Correlations have been found between the mechanical strength of capsule samples and performance in terms of perfume release in consumer applications. Having a better understanding of the key parameters that drive performance benefits the design of future formulations by offering better guidelines on the parameters that can be adjusted without worrying about the performance effects, and singles out those parameters that are essential in finding the sweet spot for capsule performance.

Keywords: consumer products, mechanical and physicochemical properties, perfume capsules, rupture behaviour

Procedia PDF Downloads 131

Authors: Munirah Ismail, Joon Hock Yeo

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Babies born with Tetralogy of Fallot, a congenital heart defect, are required to undergo reconstruction surgery to create a valved conduit. As the child matures, the partially reconstructed pulmonary conduit increases in diameter, while the size of the reconstructed valve remains the same. As a result, follow up surgery is required to replace the undersized valve. Thus, in this project, we evaluated the in-vitro performance of a bi-leaflet valve design in terms of percentage regurgitation with increasing artery (conduit) diameters. Results revealed percentage regurgitations ranging from 13% to 34% for conduits tested. It was observed that percentage of regurgitation increased exponentially with increasing diameters. While the amount of regurgitation may seem severe, it is deemed acceptable, and this valve could potentially reduce the frequency of re-operation in the lifetime of pediatric patients.

Keywords: pulmonary heart valve, tetralogy of fallot, expanded polytetrafluoroethylene valve, pediatric heart valve replacement

Procedia PDF Downloads 173

Authors: N. Amraoui, D. Hammoutene

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We have performed a theoretical study using dispersion-corrected Density Functional Methods to evaluate a variety of artificial nucleobases as candidates for metal-mediated Hoogsteen-type base pairs. We focus on A-M-T Hoogsteen-type base pair with M=Co(II), Ru(I), Ni(I). All calculations are performed using (ADF 09) program. Metal-mediated Hoogsteen-type base pairs are studied as drug candidates, their geometry optimizations are performed at ZORA/TZ2P/BLYP-D level. The molecular geometries and different energies as total energies, coordination energies, Pauli interactions, orbital interactions and electrostatic energies are determined.

Keywords: chemistry, biology, density functional method, orbital interactions

Procedia PDF Downloads 284

Authors: Reshma Jolly, Mohammad Shakir, Mohammad Shoeb Khan, Noor E. Iram

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A nanocomposite system integrating hydroxyapatite, chitin and starch (n-HA/CT/ST) has been synthesized via co-precipitation approach at room temperature, addressing the issues of biocompatibility, mechanical strength and cytotoxicity required for Bone tissue engineering. The interactions, crystallite size and surface morphology against n-HA/CT (nano-hydroxyapatite/chitin) nanocomposite have been obtained by correlating and comparing the results of FTIR, SEM, TEM and XRD. The comparative study of the bioactivity of n-HA/CT and n-HA/CT/ST nanocomposites revealed that the incorporation of starch as templating agent improved these properties in n-HA/CT/ST nanocomposite. The rise in thermal stability in n-HA/CT/ST nanocomposite as compared to n-HA/CT has been observed by comparing the TGA results. The comparison of SEM images of both the scaffolds indicated that the addition of ST influenced the surface morphology of n-HA/CT scaffold which appeared to be rougher and porous. The MTT assay on murine fibroblast L929 cells and in-vitro bioactivity of n-HA/CT/ST matrix referred superior non-toxic property of n-HA/CT/ST nanocomposite and higher possibility of osteo-integration in-vivo, respectively.

Keywords: bioactive, chitin, hyroxyapatite, nanocomposite

Procedia PDF Downloads 493

Authors: Ģirts Brasliņš, Ilja Arefjevs, Nadežda Tarakanova

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The objective of countercyclical capital buffer is to encourage banks to build up buffers in good times that can be drawn down in bad times. The aim of the report is to assess such decisions by banks derived from three approaches. The approaches are the aggregate credit-to-GDP ratio, credit growth as well as banking sector profits. The approaches are implemented for Estonia, Latvia and Lithuania for the time period 2000-2012. The report compares three approaches and analyses their relevance to the Baltic states by testing the correlation between a growth in studied variables and a growth of corresponding gaps. Methods used in the empirical part of the report are econometric analysis as well as economic analysis, development indicators, relative and absolute indicators and other methods. The research outcome is a cross-Baltic comparison of two alternative approaches to establish or release a countercyclical capital buffer by banks and their implications for each Baltic country.

Keywords: basel III, countercyclical capital buffer, banks, credit growth, baltic states

Procedia PDF Downloads 396

Authors: Dalila Oulhaci, Mohammed Zahaf

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The watering technique is essential to maintain a moist perimeter around the roots of the crop. This is the case with topical watering, where the soil around the root system can be kept permanently moist between the two extremes of water content. Moreover, one of the oldest methods used since Roman times throughout North Africa and the Near East was based on the repeated pouring of water into porous earthen vessels buried in the ground. In this context, these two techniques have been combined by replacing the earthen vase with plastic bottles filled with sand which release water through their perforated walls into the surrounding soil. The objective of this work is to first determine the purifying power of the activated sludge treatment plant of Toggourt and then that of the bottled Sawdust filter. For the station, the BOD purification rate was (96.5%), the COD purification rate was (87%) and suspended solids (90%). For the bottle, the BOD removal rate was (35%), and COD removal rate was (12.58%). This work falls within the framework of water saving, sustainable development and environmental protection, and also within the framework of agriculture.

Keywords: wasterwater, sawdust, purification, irrigation, touggourt (Algeria)

Procedia PDF Downloads 86

Authors: Makda Aamir, Sood Aayushi, Syed Omar, Nihan Khuld, Iskander Peter, Ijaz Naeem, Sharma Nishant

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Introduction:Glycogen Storage Disease Type-1 (GSD-1) is a rare phenomenon primarily affecting the liver and kidney. Excessive accumulation of glycogen and fat in liver, kidney, and intestinal mucosa is noted in patients with deficiency of Glucose-6-phosphatase deficiency. Patients with GSD-1 have a wide spectrum of symptoms, including hepatomegaly, hypoglycemia, lactic acidemia, hyperlipidemia, hyperuricemia, and growth retardation. Age of onset, rate of disease progression and its severity is variable in this disease.Case:An 18-year-old male with GSD-1a, Von Gierke’s disease, hyperuricemia, and hypertension presented to the hospital with nausea and vomiting. The patient followed an hourly cornstarch regimen during the day and overnight through infusion via a PEG tube. The complaints started at work, where he was unable to tolerate oral cornstarch. He washemodynamically stable on arrival. ABG showed pH 7.372, PaCO2 30.3, and PaO2 92.2. WBC 16.80, K+ 5.8, HCO3 13, BUN 28, Cr 2.2, Glucose 60, AST 115, ALT 128, Cholesterol 352, Triglycerides >1000, Uric Acid 10.6, Lactic Acid 11.8 which trended down to 8.0. CT abdomen showed hepatomegaly and fatty infiltration with the PEG tube in place.He was admitted to the ICU and started on D5NS for hypoglycemia and lactic acidosis. Per request by the patient’s pediatrician, he was transitioned to IV D10/0.45NS at 110mL/Hr to maintain blood glucose above 75 mg/L. Frequent accuchecks were done till he could tolerate his dietary regimen with cornstarch. Lactic acid downtrend to 2.9, and accuchecks ranged between 100-110. Cr improved to 1.3, and his home medications (Allopurinol and Lisinopril) were resumed. He was discharged in stable condition with plans for further genetic therapy work up.Discussion:Mainstay therapy for Von Gierke’s Disease is the prevention of metabolic derangements for which dietary and lifestyle changes are recommended. A low fructose and sucrose diet is recommended by limiting the intake of galactose and lactose to one serving per day. Hypoglycemia treatment in such patients is two-fold, utilizing both quick and stable release sources. Cornstarch has been one such therapy since the 1980s; its slow digestion provides a steady release of glucose over a longer period of time as compared with other sources of carbohydrates. Dosing guidelines vary from age to age and person to person, but it is highly recommended to check BG levels frequently to maintain a BG > 70 mg/dL. Associated high levels of triglycerides and cholesterol can be treated with statins, fibrates, etc. Conclusion:The management of hypoglycemia in GSD 1 disease presents various obstacles which could prove to be fatal. Due to the deficiency of G6P, treatment with a specialized hypoglycemic regimen is warranted. A D10 ½ NS infusion can be used to maintain blood sugar levels as well as correct metabolic or lactate imbalances. Infusion should be gradually weaned off after the patient can tolerate oral feeds as this can help prevent the risk of hypoglycemia and other derangements. Further research is needed in regards to these patients for more sustainable regimens.

Keywords: von gierke, glycogen storage disease, hypoglycemia, genetic disease

Procedia PDF Downloads 107

Authors: Chettou Souhaila, Soufi Omar, Roumia Mohammed Ammar

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Protecting the environment is to preserve the survival and future of humanity. Indeed, the environment is our source of food and drinking water, the air is our source of oxygen, the climate allows our survival and biodiversity are a potential drug reservoir. Preserving the environment is, therefore, a matter of survival. The objective of this project is to familiarize the general public with environmental problems not only with the theme of environmental protection, but also with the concept of biodiversity in different ecosystems. For it, the aim of our project was to create the Ecorium which is a place that preserves many species of plants of different ecosystems, schools, malls, buildings, offices, ecological transports, gardens, and many familial activities that participated in the ecosystems development, strategic biodiversity and sustainable development.

Keywords: ecological system, ecorium, environment, sustainable development

Procedia PDF Downloads 340

Authors: R. Mickiene, A. Friese, U. Rosler, A. Maruska, O. Ragazinskiene

Abstract:

This research focuses on phytochemistry and antimicrobial activities of compounds isolated and identified from three species of Eryngium. The antimicrobial activity of extracts from Eryngiumplanum L., Eryngium maritimum L., Eryngium campestre L. grown in Lithuania, were tested by the method of series dilutions, against different bacteria species: Escherichia coli, Proteus vulgaris and Staphylococcus aureus with and without antibiotic resistances, originating from livestock. The antimicrobial activity of extracts was described by determination of the minimal inhibitory concentration. Preliminary results show that the minimal inhibitory concentration range between 8.0 % and 17.0 % for the different Eryngium extracts and bacterial species.The total amounts ofphenolic compounds and total amounts of flavonoids were tested in the methanolic extracts of the plants. Identification and evaluation of the phenolic compounds were performed by liquid chromatography. The essential oils were analyzed by gas chromatography mass spectrometry.

Keywords: antimicrobial activities, Eryngium L. species, essential oils, gas chromatography mass spectrometry

Procedia PDF Downloads 447

Authors: Azita Behbahaninia

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Soil and surface and ground waters pollution to arsenic (As) due to its high potential for food cycle entrance, has high risk for human safety. Also, this pollution can cause quality and quantity decreasing of agricultural products or some lesions in farm animals that due to low knowledge, its reason is unknown, but can relate to As pollution. This study was conducted to investigate level of soil and water pollution by As in Hashtrood city. Based on the region’s information, the surface and ground waters, soil, river sediments, and rock were sampled and analyzed for physico-chemical and As in lab. There are significant differences for mean contents between As in the samples and crust. The maximum levels of As were observed in fly ash sample. Consequently, As pollution was related to geogenic and volcanic eruptions in this region. These mechanisms are diagnosed as As pollution in the region: As release for the rock units, As sorption by oxide minerals in aerobic and acidic to neutral conditions, desorption from oxide surfaces with pH increasing, increasing of As concentration in solution, and consequently pollution.

Keywords: arsenic, flyash, groundwater, soil

Procedia PDF Downloads 322

Authors: M. G. Nasuruddin, S. Ishak

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This paper deals with the traditional Malay healing ritualistic ceremony known as Main Puteri. This non-invasive intervention uses the vehicle of performance to administer the healing process. It employs the performance elements of Makyung, that is, music, movements/dance, and dramatic dialogue to heal psychosomatic maladies. There are two perspectives to this therapeutic healing process, one traditional and the other scientific. From the traditional perspective, the psychosomatic illness is attributed to the infestations/possessions by malevolent spirits. To heal such patients, these spirits must be exorcised through placating them by making offerings. From the scientific perspective, the music (sonic orders), movements (kinetic energy), and smell (olfactory) connect with the brain waves to release the chemicals that would activate the internal healing energy. Currently, in Main Puteri, the therapeutic healing ritual is no longer relevant as modern clinical medicine has proven to be more effective. Thus, Main Puteri is an anachronism in today’s technologically advanced Malaysia.

Keywords: exorcism, main puteri, shamans, therapeutic healing

Procedia PDF Downloads 355

Authors: S. Buloyan, V. Mamikonyan, H. Hakobyan, H. Harutyunyan, H. Gasparyan

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The liver is the strongest regenerating organ of the organism, and even with 2/3 surgically removed, it can regenerate completely. Hence, liver cirrhosis may only develop when the regenerating system is off. We present the results of a comparative study of structural and functional characteristics of rat liver tissue under the conditions of toxic liver cirrhosis development, induced by carbon tetrachloride, and its prevention/treatment by natural compounds with antioxidant and immune stimulating action. Studies were made on Wister rats, weighing 120~140 g. Grape seeds extracts, separately and in combination with well known anticirrhotic drug ursodeoxycholic acid (ursodiol) have demonstrated effectiveness in prevention of liver cirrhosis development and its treatment.

Keywords: carbon tetrachloride, GSE, liver cirrhosis, prevention, treatment

Procedia PDF Downloads 486

Authors: Abdulaziz Bashir Kutawa, Khairulmazmi Ahmad, Mohd Zobir Hussein, Asgar Ali, Mohd Aswad Abdul Wahab, Amara Rafi, Mahesh Tiran Gunasena, Muhammad Ziaur Rahman, Md. Imam Hossain, Syazwan Afif Mohd Zobir

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Rice is a cereal crop and belongs to the family Poaceae, it was domesticated in southern China and North-Eastern India around 8000 years ago, and it’s the staple nourishment for over half of the total world’s population. Rice production worldwide is affected by different abiotic and biotic stresses. Diseases are important challenges for the production of rice, among all the diseases in rice plants, the most severe and common disease is the rice blast. Worldwide, it is one of the most damaging diseases affecting rice cultivation, the disease is caused by the non-obligate filamentous ascomycete fungus called Magnaporthe grisae or Pyricularia oryzae Cav. Nanotechnology is a new idea to improve agriculture by combating the diseases of plants, as nanoparticles were found to possess an inhibitory effect on different species of fungi. This work aimed to develop and determine the efficacy of agronanofungicides, and commercial fungicides (in-vitro and in-vivo). The agronanofungicides were developed using ionic gelation methods. In-vitro antifungal activity of the synthesized agronanofungicides was evaluated against P. oryzae using the poisoned medium technique. The potato dextrose agar (PDA) was amended in several concentrations; 0.001, 0.005, 0.01, 0.025, 0.05, 0.1, 0.15, 0.20, 0.25, 0.30, and 0.35 ppm for the agronanofungicides. Medium with the only solvent served as a control. Mycelial growth was recorded every day, and the percentage inhibition of radial growth (PIRG) was also calculated. Based on the results of the zone of inhibition, the chitosan-hexaconazole agronanofungicide (2g/mL) was the most effective fungicide to inhibit the growth of the fungus with 100% inhibition at 0.2, 0.25, 0.30, and 0.35 ppm, respectively. The least were found to be propiconazole and basamid fungicides with 100% inhibition only at 100 ppm. In terms of the glasshouse results, the chitosan-hexaconazole-dazomet agronanofungicide (CHDEN) treatment (2.5g/L) was found to be the most effective fungicide to reduce the intensity of the disease with a disease severity index (DSI) of 19.80%, protection index (PI) of 82.26%, lesion length of 1.63cm, disease reduction (DR) of 80.20%, and AUDPC (390.60 Unit2). The least effective fungicide was found to be ANV with a disease severity index (45.60%), protection index (45.24%), lesion length (3.83 cm), disease reduction (54.40%), and AUDPC (1205.75 Unit2). The negative control did not show any symptoms during the glasshouse assay, while the untreated control treatment exhibited severe symptoms of the disease with a DSI value of 64.38%, lesion length of 5.20 cm, and AUDPC value of 2201.85 Unit2, respectively. The treatments of agronanofungicides have enhanced the yield significantly with CHDEN having 239.00 while the healthy control had 113.67 for the number of grains per panicle. The use of CHEN and CHDEN will help immensely in reducing the severity of rice blast in the fields, and this will increase the yield and profit of the farmers that produced rice.

Keywords: chitosan, dazomet, disease severity, efficacy, and blast disease

Procedia PDF Downloads 87

Authors: Agnieszka E. Laudy, Karolina Stępien, Sergiusz Lulinski, Krzysztof Durka, Stefan Tyski

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1,3-dihydro-1-hydroxy-2,1-benzoxaborole and its derivatives are a particularly interesting group of synthetic agents and were successfully employed in supramolecular chemistry medicine. The first important compounds, 5-fluoro-1,3-dihydro-1-hydroxy-2,1-benzoxaborole and 5-chloro-1,3-dihydro-1-hydroxy-2,1-benzoxaborole were identified as potent antifungal agents. In contrast, (S)-3-(aminomethyl)-7-(3-hydroxypropoxy)-1-hydroxy-1,3-dihydro-2,1-benzoxaborole hydrochloride is in the second phase of clinical trials as a drug for the treatment of Gram-negative bacterial infections of the Enterobacteriaceae family and Pseudomonas aeruginosa. Equally important and difficult task is to search for compounds active against Gram-negative bacilli, which have multi-drug-resistance efflux pumps actively removing many of the antibiotics from bacterial cells. We have examined whether halogen-substituted benzoxaborole-based derivatives and their analogues possess antibacterial activity and are substrates for multi-drug-resistance efflux pumps. The antibacterial activity of 1,3-dihydro-3-hydroxy-1,1-dimethyl-1,2,3-benzosiloxaborole and 10 halogen-substituted its derivatives, as well as 1,2-phenylenediboronic acid and 3 synthesised fluoro-substituted its analogs, were evaluated. The activity against the reference strains of Gram-positive (n=5) and Gram-negative bacteria (n=10) was screened by the disc-diffusion test (0.4 mg of tested compounds was applied onto paper disc). The minimal inhibitory concentration values and the minimal bactericidal concentration values were estimated according to The Clinical and Laboratory Standards Institute and The European Committee on Antimicrobial Susceptibility Testing recommendations. During the minimal inhibitory concentration values determination with or without phenylalanine-arginine beta-naphthylamide (50 mg/L) efflux pump inhibitor, the concentrations of tested compounds ranged 0.39-400 mg/L in the broth medium supplemented with 1 mM magnesium sulfate. Generally, the studied benzosiloxaboroles and benzoxadiboroles showed a higher activity against Gram-positive cocci than against Gram-negative rods. Moreover, benzosiloxaboroles have the higher activity than benzoxadiboroles compounds. In this study, we demonstrated that substitution (mono-, di- or tetra-) of 1,3-dihydro-3-hydroxy-1,1-dimethyl-1,2,3-benzosiloxaborole with halogen groups resulted in an increase in antimicrobial activity as compared to the parent substance. Interestingly, the 6,7-dichloro-substituted parent substance was found to be the most potent against Gram-positive cocci: Staphylococcus sp. (minimal inhibitory concentration 6.25 mg/L) and Enterococcus sp. (minimal inhibitory concentration 25 mg/L). On the other hand, mono- and dichloro-substituted compounds were the most actively removed by efflux pumps present in Gram-negative bacteria mainly from Enterobacteriaceae family. In the presence of efflux pump inhibitor the minimal inhibitory concentration values of chloro-substituted benzosiloxaboroles decreased from 400 mg/L to 3.12 mg/L. Of note, the highest increase in bacterial susceptibility to tested compounds in the presence of phenylalanine-arginine beta-naphthylamide was observed for 6-chloro-, 6,7-dichloro- and 6,7-difluoro-substituted benzosiloxaboroles. In the case of Escherichia coli, Enterobacter cloacae and P. aeruginosa strains at least a 32-fold decrease in the minimal inhibitory concentration values of these agents were observed. These data demonstrate structure-activity relationships of the tested derivatives and highlight the need for further search for benzoxaboroles and related compounds with significant antimicrobial properties. Moreover, the influence of phenylalanine-arginine beta-naphthylamide on the susceptibility of Gram-negative rods to studied benzosiloxaboroles indicate that some tested agents are substrates for efflux pumps in Gram-negative rods.

Keywords: antibacterial activity, benzosiloxaboroles, efflux pumps, phenylalanine-arginine beta-naphthylamide

Procedia PDF Downloads 271

Authors: Ahmad N. Shuid, Azri Jalil, Sabarul A. Mokhtar, Mohd F. Khamis, Norliza Muhammad

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Micro-CT provides a 3-D image of fracture callus, which can be used to calculate quantitative parameters. In this study, micro-CT was used to assess the fracture healing of orchidectomised rats, an androgen-deficient osteoporosis model. The effect of testosterone (hormone replacement) on fracture healing was also assessed with micro-CT. The rats were grouped into orchidectomised-control (ORX), sham-operated (SHAM), and orchidectomised; and injected with testosterone intramuscularly once weekly (TEN). Treatment duration was six weeks. The fracture was induced and fixed with plates and screws in the right tibia of all the rats. An in vitro micro-CT was used to scan the fracture callus area which consisted of 100 axial slices above and below fracture line. The analysis has shown that micro-CT was able to detect a significant difference in the fracture healing rate of ORX and TEN groups. In conclusion, micro-CT can be used to assess fracture healing in androgen-deficient osteoporosis. This imaging tool can be used to test agents that influence fracture healing in the androgen-deficient model.

Keywords: androgen, fracture, orchidectomy, osteoporosis

Procedia PDF Downloads 545