Search results for: ethyl ester

Authors: P. H. Mfengwana, S. S. Mashele, L. Verschaeve, R. Anthonissen, I. T. Manduna

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Gunnera perpensa is traditionally used mostly by women for the treatment of different gynaecological related conditions due to its proven uterine contractility effects. The uses of this plant include menstrual pain relief, treatment of infertility and promotion of easy labour. However, even though this plant species has been reported to possess numerous medicinal properties, to author’s best knowledge, its safety has not been investigated. Thus, this study was aimed at investigating the genotoxicity and antigenotoxicity of Gunnera perpensa aqueous, methanol and dichloromethane extracts. The in vitro toxicity of the plant extracts was assessed with the neutral red uptake (NRU) test. Genotoxic and antigenotoxic properties of Gunnera perpensa were investigated using high-throughput assays: bacterial Vitotox test and the alkaline comet assay with and without S9 activation on human C3A cells. Ethyl Methanesulfonate (EMS) and 4-nitroquinoline-oxide (4-NQO) were used as positive controls, respectively. All extracts showed toxicity in a dose-dependent manner; however, that does not mean they were all genotoxic. Methanol extract did show genotoxicity with S9 (metabolism) only at the highest concentration of 500 µg/ml due to increased DNA damage observed, however, no genotoxicity was observed from other concentrations. Therefore, the results show that Gunnera perpensa extracts are genotoxic and not safe for human use.

Keywords: antigenotoxicity, comet test, genotoxicity, Gunnera perpensa, vitotox assay

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Authors: Rohit Singh Dangi, Ravi Kant Pal, Monica Sundd

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Acyl-CoA binding protein (ACBP) is a housekeeping protein which functions as an intracellular carrier of acyl-CoA esters. Given the fact that the amastigote stage (blood stage) of Leishmania depends largely on fatty acids as the energy source, of which a large part is derived from its host, these proteins might have an important role in its survival. In Leishmania major, genome sequencing suggests the presence of six ACBPs, whose function remains largely unknown. For functional and structural characterization, one of the ACBP genes was cloned, and the protein was expressed and purified heterologously. Acyl-CoA ester binding and stoichiometry were analyzed by isothermal titration calorimetry and Dynamic light scattering. Our results shed light on high affinity of ACBP towards longer acyl-CoA esters, such as myristoyl-CoA to arachidonoyl-CoA with single binding site. To understand the binding mechanism & dynamics, Nuclear magnetic resonance assignments of this protein are being done. The protein's crystal structure was determined at 1.5Å resolution and revealed a classical topology for ACBP, containing four alpha-helical bundles. In the binding pocket, the loop between the first and the second helix (16 – 26AA) is four residues longer from other extensively studied ACBPs (PfACBP) and it curls upwards towards the pantothenate moiety of CoA to provide a large tunnel space for long acyl chain insertion.

Keywords: acyl-coa binding protein (ACBP), acyl-coa esters, crystal structure, isothermal titration, calorimetry, Leishmania

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Authors: Jisoo Kim, Min Su Lee, Sunmook Lee

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Durability assessment of nanocomposite-based bone fixation device was performed by flexural fatigue tests, for which the changes in the life cycles of nanocomposite samples synthesized by blending bioabsorbable polymer (PLGA) and ceramic nanoparticles (β-TCP) with different ratios were monitored. The nanocomposite samples were kept in a constant temperature/humidity chamber at 37°C/50%RH for varied incubation periods for the degradation of nanocomposite samples under the temperature/humidity stress. It was found that the life cycles were increasing as the incubation time in the chamber were increasing in the initial stage irrespective of sample compositions, which was due to the annealing effect of the polymer. However, the life cycle was getting shorter as the incubation time increased afterward, which was due to the overall degradation of nanocomposites. It was found that the life cycle of the nanocomposite sample with high ceramic content was shorter than the one with low ceramic content, which was attributed to the increased brittleness of the composite with high ceramic content. The changes in chemical properties were also monitored by FT-IR, which indicated that the degradation of the biodegradable polymer could be confirmed by the increased intensities of carboxyl groups and hydroxyl groups since the hydrolysis of ester bonds connecting two successive monomers yielded carboxyl end groups and hydroxyl groups.

Keywords: bioabsorbable polymer, bone fixation device, ceramic nanoparticles, durability assessment, fatigue test

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Authors: S. Techaoei, K. Jarmkom, P. Eakwaropas, W. Khobjai

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The objective of this research was focused on investigating in vitro antimicrobial activity of Phellinus linteus fruiting body extracts on Pseudomonas aeruginosa, Escherichia coli, Staphylococcus aureus and Methicillin-resistant Staphylococcus aureus. Phellinus linteus fruiting body was extracted with ethanol and ethyl acetate and was vaporized. The disc diffusion assay was used to assess antimicrobial activity against tested bacterial strains. Primary screening of chemical profile of crude extract was determined by using thin layer chromatography. The positive control and the negative control were used as erythromycin and dimethyl sulfoxide, respectively. Initial screening of Phellinus linteus crude extract with the disc diffusion assay demonstrated that only ethanol had greater antimicrobial activity against Pseudomonas aeruginosa, Escherichia coli, Staphylococcus aureus and Methicillin-resistant Staphylococcus aureus. The MIC assay showed that the lower MIC was observed with 0.5 mg/ml of Pseudomonas aeruginosa and Methicillin-resistant Staphylococcus aureus and 0.25 mg/ml. of Escherichia coli and Staphylococcus aureus, respectively. TLC chemical profile of extract was represented at R_f ≈ 0.71-0.76.

Keywords: Staphylococcus aureus, Escherichia coli, Phellinus linteus, Methicillin-resistant Staphylococcus aureus, antimicrobial activity

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Authors: Habib Alah Dadgar, Nasim Norouzbeigi

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The precise definition margin of high and low-grade gliomas is crucial for treatment. We aimed to assess the feasibility of assessment of the resection legions with post-operative positron emission tomography (PET) using [18F]O-(2-[18F]-fluoroethyl)-L-tyrosine ([18F]FET). Four patients with the suspicion of high and low-grade were enrolled. Patients underwent post-operative [18F]FET-PET, pre-operative magnetic resonance imaging (MRI) and CT for clinical evaluations. In our study, three patients had negative response to recurrence and progression and one patient indicated positive response after surgery. [18F]FET-PET revealed a legion of increased radiotracer uptake in the dura in the craniotomy site for patient 1. Corresponding to the patient history, the study was negative for recurrence of brain tumor. For patient 2, there was a lesion in the right parieto-temporal with slightly increased uptake in its posterior part with SUVmax = 3.79, so the study was negative for recurrence evaluation. In patient 3 there was no abnormal uptake with negative result for recurrence of brain tumor. Intense radiotracer uptake in the left parietal lobe where in the MRI there was a lesion with no change in enhancement in the post-contrast image is indicated in patient 4. Assessment of the resection legions in high and low-grade gliomas with [18F]FET-PET seems to be useful.

Keywords: FET-PET, CT, glioma, MRI

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Authors: Ehab El-Dabaa, Omnia Ali, Mohamed Abd El-Hady, Ahmed Osman

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Recombinant human interferon alpha 2 (rhIFN-α2) is FDA approved for treatment of some viral and malignant diseases. Approved pegylated rhIFN-α2 drugs have highly improved pharmacokinetics, pharmacodynamics and therapeutic efficiency compared to native protein. In this work, we studied the pegylation of purified properly refolded rhIFN-α2b using linear 20kDa PEG-NHS (polyethylene glycol- N-hydroxysuccinimidyl ester) to prepare pegylated rhIFN-α2b with high stability and activity. The effect of different parameters like rhIFN-α2b final concentration, pH, rhIFN-α2b/PEG molar ratios and reaction time on the efficiency of pegylation (high percentage of monopegylated rhIFN-α2b) have been studied in small scale (100µl) pegylation reaction trials. Study of the percentages of different components of these reactions (mono, di, polypegylated rhIFN-α2b and unpegylated rhIFN-α2b) indicated that 2h is optimum time to complete the reaction. The pegylation efficiency increased at pH 8 (57.9%) by reducing the protein concentration to 1mg/ml and reducing the rhIFN-α2b/PEG ratio to 1:2. Using larger scale pegylation reaction (65% pegylation efficiency), ion exchange chromatography method has been optimized to prepare and purify the monopegylated rhIFN-α2b with high purity (96%). The prepared monopegylated rhIFN-α2b had apparent Mwt of approximately 65 kDa and high in vitro antiviral activity (2.1x10⁷ ± 0.8 x10⁷ IU/mg). Although it retained approximately 8.4 % of the antiviral activity of the unpegylated rhIFN-α2b, its activity is high compared to other pegylated rhIFN-α2 developed by using similar approach or higher molecular weight branched PEG.

Keywords: antiviral activity, rhIFN-α2b, pegylation, pegylation efficiency

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Authors: Shuofeng Yuan, Bojian Zheng

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Assembly of the heterotrimeric polymerase complex of influenza virus from the individual subunits PB1, PA, and PB2 is a prerequisite for viral replication, in which the interaction between the N-terminal of PB1 (PB1N) and the C terminal of PA (PAC) may be a desired target for antiviral development. In this study, we first compared the feasibility of high throughput screening by enzyme-linked immunosorbent assay (ELISA) and fluorescence polarization (FP) assay. Among the two, ELISA was demonstrated to own broader dynamic range so that it was used for screening inhibitors, which blocked PA and PB1 interaction. Several binding inhibitors of PAC-PB1N were identified and subsequently tested for the antiviral efficacy. Apparently, 3-(2-chlorophenyl)-6-ethyl-7-methyl[1,2,4]triazolo[4,3-a]pyrimidin-5-ol, designated ANA-1, was found to be a strong inhibitor of PAC-PB1N interaction and act as a potent antiviral agent against the infections of multiple subtypes of influenza A virus, including H1N1, H3N2, H5N1, H7N7, H7N9 and H9N2 subtypes, in cell cultures. Intranasal administration of ANA-1 protected mice from lethal challenge and reduced lung viral loads in H1N1 virus infected BALB/c mice. Docking analyses predicted that ANA-1 bound to an allosteric site of PAC, which would cause conformational changes thereby disrupting the PAC-PB1N interaction. Overall, our study has identified a novel compound with potential to be developed as an anti-influenza drug.

Keywords: influenza, antiviral, viral polymerase, compounds

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Authors: Y. A. Shapovalov, F. M. Gumerov, M. K. Nauryzbaev, S. V. Mazanov, R. A. Usmanov, A. V. Klinov, L. K. Safiullina, S. A. Soshin

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A flow-through installation was created and manufactured for the transesterification of triglycerides of fatty acids and production of biodiesel fuel under supercritical fluid conditions. Transesterification of rapeseed oil with ethanol was carried out according to two parameters: temperature and the ratio of alcohol/oil mixture at the constant pressure of 19 MPa. The kinetics of the yield of fatty acids ethyl esters (FAEE) was determined in the temperature range of 320-380 °C at the alcohol/oil molar ratio of 6:1-20:1. The content of the formed FAEE was determined by the method of correlation of the resulting biodiesel fuel by its kinematic viscosity. The maximum FAEE yield (about 90%) was obtained within 30 min at the ethanol/oil molar ratio of 12:1 and a temperature of 380 °C. When studying of transesterification of triglycerides, a kinetic model of an isothermal flow reactor was used. The reaction order implemented in the flow reactor has been determined. The first order of the reaction was confirmed by data on the conversion of FAEE during the reaction at different temperatures and the molar ratios of the initial reagents (ethanol/oil). Using the Arrhenius equation, the values of the effective constants of the transesterification reaction rate were calculated at different reaction temperatures. In addition, based on the experimental data, the activation energy and the pre-exponential factor of the transesterification reaction were determined.

Keywords: biodiesel, fatty acid esters, supercritical fluid technology, transesterification

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Authors: Ieva Gaide, Violeta Makareviciene

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Increasing environmental pollution is caused by various factors, including the usage of vehicles. Legislation is focused on the increased usage of renewable energy sources for fuel production. Electric car usage is also important; however, it is relatively new and expensive transport. It is necessary to increase the amount of renewable energy in the production of diesel fuel, whereas many agricultural machineries are powered by diesel, as are water vehicles. For this reason, research on biodiesel production is relevant. The majority of studies globally are related to the improvement of conventional biofuel production technologies by applying the transesterification process of oil using alcohol and catalyst. Some of the more recent methods to produce biodiesel are based on heterogeneous catalysis, which has the advantage of easy separation of catalyst from the final product. It is known that a large amount of eggshells is treated as waste; therefore, it is eliminated in landfills without any or with minimal pre-treatment. CaO, which is known as a good catalyst for biodiesel synthesis, is a key component of eggshells. In the present work, we evaluated the catalytic efficiency of eggshells and determined the optimal transesterification conditions to obtain biodiesel that meets the standards. Content CaO in eggshells was investigated. Response surface methodology was used to determine the optimal reaction conditions. Three independent variables were investigated: the molar ratio of alcohol to oil, the amount of the catalyst, and the duration of the reaction. It was obtained that the optimum transesterification conditions when the methanol and eggshells as a heterogeneous catalyst are used and the process temperature is 64°C are the following: the alcohol-to-oil molar ratio 10.93:1, the reaction duration 9.48 h, and the catalyst amount 6.80 wt%. Under these conditions, 97.79 wt% of the ester yield was obtained.

Keywords: heterogeneous catalysis, eggshells, biodiesel, oil

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Authors: Priyanka Sharma, Niti Puri

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Anemia develops when blood lacks enough healthy erythrocytes. Past studies indicated that anemia, inflammatory process, and oxidative stress are interconnected. Erythrocytes are continuously exposed to reactive oxygen species (ROS) during circulation, due to normal aerobic cellular metabolism and also pathology of inflammatory diseases. Systemic mastocytosis and genetic depletion of mast cells have been shown to affect anaemia. In the present study, we attempted to reveal whether mast cells have a direct role in clearance or erythrophagocytosis of normal or oxidatively damaged erythrocytes. Murine erythrocytes were treated with tert-butyl hydroperoxidase (t-BHP), an agent that induces oxidative damage and mimics in vivo oxidative stress. Normal and oxidatively damaged erythrocytes were labeled with carboxyfluorescein succinimidyl ester (CFSE) to track erythrophagocytosis. We show, for the first time, direct erythrophagocytosis of oxidatively damaged erythrocytes in vitro by RBL-2H3 mast cells as well as in vivo by murine peritoneal mast cells. Also, activated mast cells, as may be present in inflammatory conditions, showed a significant increase in the uptake of oxidatively damaged erythrocytes than resting mast cells. This suggests the involvement of mast cells in erythrocyte clearance during oxidative stress or inflammatory disorders. Partial inhibition of phagocytosis by various inhibitors indicated that this process may be controlled by several pathways. Hence, our study provides important evidence for involvement of mast cells in severe anemia due to inflammation and oxidative stress and might be helpful to circumvent the adverse anemic disorders.

Keywords: mast cells, anemia, erythrophagocytosis, oxidatively damaged erythrocytes

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Authors: Nouria Bouchikhi, Soufiane Bedjaoui, C. Tewfik Bouchaour, Lamia Alachaher Bedjaoui, Ulrich Maschke

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Swelling properties and phase diagrams of binary systems composed of liquid crystalline networks and a low molecular mass liquid crystal (LMWLC) have been investigated. The networks were prepared by ultraviolet (UV) irradiation of reactive mixtures including a monomer, a cross-linking agent and a photo-initiator. These networks were prepared using two cross-linking agents: 1,6 hexanedioldiacrylate (HDDA) and a mesogenic acrylic acid 6-(4’-(6-acryloyloxy-hexyloxy) biphenyl-4-yl oxy) hexyl ester (AHBH). The obtained dry networks were characterized by differential scanning calorimetry, and immersed in an excess of a LMWLC solvent 4-cyano-4’-pentylbiphenyl (5CB), forming polymer gels. A detailed study by polarized optical microscopy allowed to determine the swelling degree of the gels and to follow the phase behavior of the solvent inside the polymer matrix in a wide range of temperature. It has been found that the gels undergo a sharp decrease of their swelling degree in response to an infinitesimal change of temperature. This finding adds new and interesting aspects on the actuators applications. We have subsequently explored the effect of different parameters on volume phase transition of these liquid crystalline materials. Such as the cross-linking density (CD), a nature of cross-linking agent and the photo initiator concentration.

Keywords: cross-linking density, liquid crystalline elastomers, phase diagrams, swelling

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Authors: Polina Prokopovich

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Disease-modifying osteoarthritis drugs (DMOADs) are a new therapeutic class for OA, preventing or inhibiting OA development. Unfortunately, none of the DMOADs have been clinically approved due to their poor therapeutic effects in clinical trials. The joint environment has played a role in the poor clinical performance of these drugs by limiting the amount of drug effectively delivered as well as the time that the drug spends within the joint space. The current study aims to enhance the cartilage uptake and retention time of the DMOADs-model (licofelone), which showed a significant therapeutic effect against OA progression and is currently in phase III. Licofelone will be covalently conjugated to the hydrolysable, cytocompatible, and cationic poly beta-amino ester polymers (PBAE). The cationic polymers (A16 and A87) can be electrostatically attached to the negatively charged cartilage component (glycosaminoglycan), which will increase the drug penetration through the cartilage and extend the drug time within the cartilage. In the cartilage uptake and retention time studies, an increase of 18 to 37 times of the total conjugated licofelone to A87 and A16 was observed when compared to the free licofelone. Furthermore, the conjugated licofelone to A87 was detectable within the cartilage at 120 minutes, while the free licofelone was not detectable after 60 minutes. Additionally, the A87-licofelone conjugate showed no effect on the chondrocyte viability. In conclusion, the cationic A87 and A16 polymers increased the percentage of licofelone within the cartilage, which could potentially enhance the therapeutic effect and pharmacokinetic performance of licofelone or other DMOADs clinically.

Keywords: PBAE, cartilage., osteoarthritis, injectable biomaterials, drug delivery

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Authors: Kunle Oni

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This study investigated the bioactivity potentials of porridge from yellow maize and malted sorghum enriched with Cirinaforda.All the samples were analyzed using standard methods.Results showed that the highest value 217.03μmolTEAC/100g, 43.3 mmol Fe2+ /100g, and 35.56% for DPPH, FRAP and TBARS respectively were reported in sample 50FYM+20MS+30CF, while the lowest value 146.10μmolTEAC/100, 20.18±0.11 mmol Fe2+/100g and 13.25% for DPPH, FRAP and TBARS were reported in the control sample.The oxalate and tannin contents were lowest in sample 50FYM+20MS+30CFbutOxalate was highest in the control sample while tannin was highest in sample 60FYM+20MS+20CF.The phytate content was highest in the 60FYM+20MS+20CF mixture (2.32 mg/100g) and lowest in the control (100% FYM) porridge (2.20 mg/100g).The result also showed that the total phenolic content was highest in the 60FYM+20MS+20CF mixture (318.28 mg GAE/100g) and lowest in the50FYM+30MS+20CF mixture (264.18mg GAE/100g).The total flavonoid content had the50FYM+20MS+30CFmixture having the highest content (189.31mg RE/100g) and the 60FYM+20MS+20CF mixture having the lowest (90.10mg RE/100g). The enrichment of the porridge with C. fordaincreased the concentration of various bioactive compounds compared to the control sample. The identified compounds cinnamic acid, methyl ester, 10-Methyl-E-11-tridecen-1-ol propionate, methaqualone,3-(2-Hydroxy-6-methylphenyl)-4(3H)-quinazolinone, and oleic acid

Keywords: bioactive compounds, characterization, cereal-based porridge, Cirina forda

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Authors: Gabriel S. De Oliveira, Patricia P. Adriani, Christophe Moriseau, Bruce D. Hammock, Felipe S. Chambergo

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Epoxide hydrolases (EHs) are enzymes that are present in all living organisms and catalyze the hydrolysis of epoxides to the corresponding vicinal diols. EHs have high biotechnological interest for the drug design and chemistry transformation for industries. In this study, we describe the identification of substrates and inhibitors of epoxide hydrolase enzyme from the filamentous fungus Trichoderma reesei (TrEH), and these inhibitors showed the fungal growth inhibitory activity. We have used the cloned enzyme and expressed in E. coli to develop the screening in the library of fluorescent substrates with the objective of finding the best substrate to be used in the identification of good inhibitors for the enzyme TrEH. The substrate (3-phenyloxiranyl)-acetic acid cyano-(6-methoxy-naphthalen-2-yl)-methyl ester showed the highest specific activity and was chosen for the next steps of the study. The inhibitors screening was performed in the library with more than three thousand molecules and we could identify the 6 best inhibitors. The IC50 of these molecules were determined in nM and all the best inhibitors have urea or amide in their structure, because It has been recognized that these groups fit well in the hydrolase catalytic pocket of the epoxide hydrolases. Then the growth of T. reesei in PDA medium containing these TrEH inhibitors was tested, and fungal growth inhibition activity was demonstrated with more than 60% of inhibition of fungus growth in the assay with the TrEH inhibitor with the lowest IC50. Understanding how this EH enzyme from T. reesei responds to inhibitors may contribute for the study of fungal metabolism and drug design against pathogenic fungi.

Keywords: epoxide hydrolases, fungal growth inhibition, inhibitor, Trichoderma reesei

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Authors: Ahmed Jibrin Uttu, Maimuna Waziri

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The root bark of Glossonema boveanum (Decne), a member of Apocynaceae family, is used by traditional medicine practitioner to treat urinary and respiratory tract infections, bacteremia, typhoid fever, bacillary dysentery, diarrhea and stomach pain. This present study aims to validate the medicinal claims ascribed to the root bark of the plant. Preliminary phytochemical study of the root bark extracts (n-hexane, ethyl acetate, chloroform and methanol extracts) showed the presence of alkaloids, carbohydrates, steroids, triterpenes, cardiac glycosides, saponins, tannins and flavonoids. Antimicrobial study of the extracts showed activities against Staphylococus aureus, Bacillus subtilis, Salmonella typhii, Shigella dysenteriae, Escherichia coli, Enterobacter cloacae, Streptococcus agalactiae and Candida albicans while Micrococcus luteus, Pseudomonas aeruginosa and Klebsiella Pneumoniae showed resistance to all the extracts. The inhibitory effect was compared with the standard drug ciprofloxacin and fluconazole. MIC and MBC for both extracts were also determined using the tube dilution method. This study concluded that the root bark of G. boveanum, used traditionally as a medicinal plant, has antimicrobial activities against some causative organisms.

Keywords: Glossonema boveanum (Decne.), phytochemical, antimicrobial, minimum inhibitory concentration, minimum bactericidal concentration

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Authors: Dagim Ali Hussen, Adnan A. Bekhit, Ariaya Hymete

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In this study, several pyridine derivatives were synthesized and evaluated for their in vitro antimicrobial activity against gram-positive bacteria (S. aureus and B. Cereus), gram-negative bacteria (P. aeruginosa and E. coli) and fungus (C. albican and A niger). The intermediate chalcone derivative 2a,b was synthesized by condensation of pyrazole aldehydes 1a,b with acetophenone in alcoholic KOH. Cyclization of 2a,b with ethyl cyanoacetate ad ammonium acetate resulted in pyridine carbonitrile derivatives 3a,b. Furthermore, condensation of pyridine-4-carboxaldeyhe with different amino-derivatives gave rise to pyridine derivatives 5a,b, 6a,b. The oxadiazole derivative 7a was prepared by cyclization of 6a with acetic anhydride. Characterization of the synthesized compound was performed using IR, 1H NMR, 13C NMR spectra and elemental microanalyses. The antimicrobial results revealed that compounds 5a, 6b and 7a exhibited half fold antibacterial activity compared to ampicillin, against B. cereus. On the other hand, compound 3b showed an equivalent activity compared to miconazole against candida albican (CANDAL 03) and to clotrimazole against the clinical isolate candida albican 6647. Moreover, this compound 3b was further tested for its acute toxicity profile. The results showed that oral LD50 is more that 300 mg/kg and parentral LD50 is more than 100 mg/kg. Compound 3b is a good candidate for antifungal agent with good toxicity profile, and deserves more chemical derivatization and clinical study.

Keywords: antifungal, antimicrobial, Candida albican, pyridine

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Authors: Li Lin Ong, Duc Thinh Khong, Zaher M. A. Judeh

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Phenylpropanoid sucrose esters (PSEs) are natural compounds found in various medicinal plants which exhibit important biological activities such as antiproliferation and α- and β-glucosidase inhibitory activities. Despite their potential as new therapeutics, total synthesis of PSEs has been very limited as their inherent structures contain one or more (substituted) cinnamoyl groups randomly allocated on the sucrose core via ester linkage. Since direct acylation of unprotected sucrose would be complex and tedious due to the presence of eight free hydroxyl groups, partially protected 2,1’:4,6-di-O-diisopropylidene sucrose was used as the starting material instead. However, similar reactivity between the remaining four hydroxyl groups still pose a challenge in the total synthesis of PSEs as the lack of selectivity can restrict customisation where acylation at specific OH is desired. To overcome this problem, a 4-step orthogonal protection scheme was developed. In this scheme, the remaining four hydroxyl groups on 2,1’:4,6-di-O-diisopropylidene sucrose, 6’-OH, 3’-OH, 4’-OH, and 3-OH, were protected with different protecting groups with an overall yield of > 40%. This orthogonally protected intermediate would provide a convenient and divergent access to a wider range of natural and synthetic PSEs as (substituted) cinnamoyl groups can be selectively introduced at desired positions. Using this scheme, three different series of monosubstituted PSEs were successfully synthesized where (substituted) cinnamoyl groups were introduced selectively at O-3, O-3’, and O-4’ positions, respectively. The expanded library of PSEs would aid in structural-activity relationship study of PSEs for identifying key components responsible for their biological activities.

Keywords: orthogonal protection, phenylpropanoid sucrose esters, selectivity, sucrose

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Authors: M. Masłowski, M. Zaborski

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Magnetorheological elastomer composites based on micro- and nano-sized Fe3O4 magnetoactive fillers in silicone rubber are reported and studied. To improve the dispersion of applied fillers in polymer matrix, ionic liquids such as 1-ethyl-3-methylimidazolium diethylphosphate, 1-butyl-3-methylimidazolium hexafluorophosphate, 1-hexyl-3-methylimidazolium chloride, 1-butyl-3-methylimidazolium trifluoromethanesulfonate,1-butyl-3-methylimidazolium tetrafluoroborate, trihexyltetradecylphosphonium chloride were added during the process of composites preparation. The method of preparation process influenced the specific properties of MREs (isotropy/anisotropy), similarly to ferromagnetic particles content and theirs quantity. Micro and non-sized magnetites were active fillers improving the mechanical properties of elastomers. They also changed magnetic properties and reinforced the magnetorheological effect of composites. Application of ionic liquids as dispersing agents influenced the dispersion of magnetic fillers in the elastomer matrix. Scanning electron microscopy images used to observe magnetorheological elastomer microstructures proved that the dispersion improvement had a significant effect on the composites properties. Moreover, the particles orientation and their arrangement in the elastomer investigated by vibration sample magnetometer showed the correlation between MRE microstructure and their magnetic properties.

Keywords: magnetorheological elastomers, iron oxides, ionic liquids, dispersion

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Authors: R. Tajau, R. Rohani, M. S. Alias, N. H. Mudri, K. A. Abdul Halim, M. H. Harun, N. Mat Isa, R. Che Ismail, S. Muhammad Faisal, M. Talib, M. R. Mohamed Zin

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Bio-based polymeric materials are increasingly used for a variety of applications, including surface coating, drug delivery systems, and tissue engineering. These polymeric materials are ideal for the aforementioned applications because they are derived from natural resources, non-toxic, low-cost, biocompatible, and biodegradable, and have promising thermal and mechanical properties. The nature of hydrocarbon chains, carbon double bonds, and ester bonds allows various sources of oil (edible), such as soy, sunflower, olive, and oil palm, to fine-tune their particular structures in the development of innovative materials. Palm oil can be the most eminent raw material used for manufacturing new and advanced natural polymeric materials involving radiation techniques, such as coating resins, nanoparticles, scaffold, nanotubes, nanocomposites, and lithography for different branches of the industry in countries where oil palm is abundant. The radiation technique is among the most versatile, cost-effective, simple, and effective methods. Crosslinking, reversible addition-fragmentation chain transfer (RAFT), polymerisation, grafting, and degradation are among the radiation mechanisms. Exposure to gamma, EB, UV, or laser irradiation, which are commonly used in the development of polymeric materials, is used in these mechanisms. Therefore, this review focuses on current radiation processing technologies for the development of various radiation-curable bio-based polymeric materials with a promising future in biomedical and industrial applications. The key focus of this review is on radiation curable palm oil-based products, which have been published frequently in recent studies.

Keywords: palm oil, radiation processing, surface coatings, VOC

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Authors: Umran Kurtan, Hamide Aydin, Sevim Unugur Celik, Ayhan Bozkurt

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In the present work, novel hBN/polyacrylonitrile composite nanofibers were produced via electrospinning approach and loaded with the electrolyte for rechargeable lithium-ion battery applications. The electrospun nanofibers comprising various hBN contents were characterized by using Fourier transform infrared spectroscopy (FT-IR), thermogravimetric analysis (TGA), X-ray diffraction (XRD) and scanning electron microscopy (SEM) techniques. The influence of hBN/PAN ratios onto the properties of the porous composite system, such as fiber diameter, porosity, and the liquid electrolyte uptake capability were systematically studied. Ionic conductivities and electrochemical characterizations were evaluated after loading electrospun hBN/PAN composite nanofiber with liquid electrolyte, i.e., 1 M lithium hexafluorophosphate (LiPF6) in ethylene carbonate (EC)/ethyl methyl carbonate (EMC) (1:1 vol). The electrolyte loaded nanofiber has a highest ionic conductivity of 10−3 S cm⁻¹ at room temperature. According to cyclic voltammetry (CV) results it exhibited a high electrochemical stability window up to 4.7 V versus Li+/Li. Li//10 wt% hBN/PAN//LiCO₂ cell was produced which delivered high discharge capacity of 144 mAhg⁻¹ and capacity retention of 92.4%. Considering high safety and low cost properties of the resulting hBN/PAN fiber electrolytes, these materials can be suggested as potential separator materials for lithium-ion batteries.

Keywords: hexagonal boron nitride, polyacrylonitrile, electrospinning, lithium ion battery

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Authors: Vania Helena Tonussi Vidal, Ester Eliane Jeunon

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This article aims to analyze the change processes of management related bureaucracy and learning organization model. The theoretical framework was based on Beer and Nohria (2001) model, identified as E and O Theory. Based on this theory the empirical research was conducted in connection with six key dimensions: goal, leadership, focus, process, reward systems and consulting. We used a case study of an educational Institution located in Barbacena, Minas Gerais. This traditional center of technical knowledge for long time adopted the bureaucratic way of management. After many changes in a business model, as the creation of graduate and undergraduate courses they decided to make a deep change in management model that is our research focus. The data were collected through semi-structured interviews with director, managers and courses supervisors. The analysis were processed by the procedures of Collective Subject Discourse (CSD) method, develop by Lefèvre & Lefèvre (2000), Results showed the incremental growing of management model toward a learning organization. Many impacts could be seeing. As negative factors we have: people resistance; poor information about the planning and implementation process; old politics inside the new model and so on. Positive impacts are: new procedures in human resources, mainly related to manager skills and empowerment; structure downsizing, open discussions channel; integrated information system. The process is still under construction and now great stimulus is done to managers and employee commitment in the process.

Keywords: bureaucracy, organizational learning, organizational change, E and O theory

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Authors: Lamees A. Ben Saad, Kah Hwi Kim, Chin Chew Quah, Mustafa Shahimi

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Background: Punica granatum (pomegranate) was used as a traditional medicine in different parts of the world. It has been used in the treatment of pain and inflammatory conditions such as peptic ulcer. The numerous risks associated with nonsteroidal anti-inflammatory drugs (NSAIDs) for the treatment of pain and inflammation give rise to using medicinal herbs as alternative therapies. This study aimed to evaluate the anti-inflammatory effect of the ethyl acetate pomegranate fraction (EtOAc) by determination of its inhibitory effects on lipopolysaccharide (LPS), stimulated nitric oxide (NO), prostaglandin E2 (PGE-2), interleukin-6 (IL-6) and cyclooxxgenase-2 (COX2) release from RAW264.7cells. Methods: The inhibitory effect of EtOAc was evaluated on (LPS) induced NO production, PGE2, and IL-6 quantified by immunoassay kit and prostaglandin E2 competitive ELISA kit. COX2 production is an in vitro indication of possible anti-inflammatory activity and was estimated by Western blotting. Results: EtOAc potentially inhibited LPS-induced nitric oxide, prostaglandin, and IL-6 production. With these findings, it was evident that the EtOAc could reduce the LPS-induced cyclooxygenase-2 (COX-2) at the protein level in a dose-dependent manner as determined by Western blotting. Conclusion: The results emphasize potential therapeutic applications of Punica granatum in the treatment of inflammation.

Keywords: inflammation, Punica granatum, cytotoxicity, cytokines

Procedia PDF Downloads 634

Authors: S. S. Patil, R. M. Mhetre, S. V. Patil

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Lisinopril is an angiotensin converting enzyme inhibitor used in the treatment of hypertension and heart failure in prophylactic treatment after myocardial infarction and in diabetic nephropathy. However, it is very poorly absorbed from gastro-intestinal tract. Intranasal administration is an ideal alternative to the parenteral route for systemic drug delivery. Formulating multiparticulate system with mucoadhesive polymers provide a significant increase in the nasal residence time. The aim of the present approach was to overcome the drawbacks of the conventional dosage forms of lisinopril by formulating intranasal microspheres with Carbopol 974P NF and HPMC K4 M along with film forming polymer ethyl cellulose.The microspheres were prepared by emulsion solvent evaporation method. The prepared microspheres were characterized for encapsulation efficiency, drug loading, particle size, and surface morphology, degree of swelling, ex vivo mucoadhesion, drug release, ex vivo diffusion studies. All formulations has shown entrapment efficiency between 80 to more than 95%, mucoadhesion was more than 80 % and drug release up to 90 %. Ex vivo studies revealed tht the improved bioavailability of drug compared to oral drug administration. Both in vitro and in vivo studies conclude that combination of Carbopol and HPMC based microspheres shown better results than single carbopol based microspheres for the delivery of lisinopril.

Keywords: microspheres, lisinopril, nasal delivery, solvent evaporation method

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Authors: Emily Schlebes, Christian Hundhausen, Jens W. Fischer

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The glycosaminoglycan hyaluronan (HA) is a major component of the extracellular matrix, typically produced by fibroblasts of the connective tissue but also by immune cells. Here, we investigated the capacity of human peripheral blood CD8 T cells from healthy donors to produce HA and to express HA receptors as well as HA degrading enzymes. Further, we evaluated the effect of pharmacological HA inhibition on CD8 T cell function. Using immunocytochemistry together with quantitative PCR analysis, we found that HA synthesis is rapidly induced upon antibody-induced T cell receptor (TCR) activation and almost exclusively mediated by HA synthase 3 (HAS3). TCR activation also resulted in the upregulation of HA receptors CD44, hyaluronan-mediated motility receptor (HMMR), and layilin (LAYN), although kinetics and strength of expression varied greatly between subjects. The HA-degrading enzymes HYAL1 and HYAL2 were detected at low levels and induced by cell activation in some individuals. Interestingly, expression of HAS3, HA receptors, and hyaluronidases were modulated by the proinflammatory cytokines IL-6 and IL-1bβ in most subjects. To assess the functional role of HA in CD8 T cells, we performed carboxyfluorescein succinimidyl ester (CFSE) based proliferation assays and cytokine analysis in the presence of the HA inhibitor 4- Methylumbelliferone (4-MU). Despite significant inter-individual variation with regard to the effective dose, 4-MU resulted in the inhibition of CD8 T cell proliferation and reduced release of TNF-α and IFN-γ. Collectively, these data demonstrate that human CD8 T cells respond to TCR stimulation with a synthesis of HA and expression of HA-related genes. They further suggest that HA inhibition may be helpful in interfering with pathogenic T cell activation in human disease.

Keywords: CD8 T cells, extracellular matrix, hyaluronan, hyaluronan synthase 3

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Authors: Swati Bishnoi, D. Haranath, Vinay Gupta

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In this work, we demonstrate that the power conversion efficiency (PCE) of organic solar cells (OSCs) could be improved significantly by using ZnO doped with Aluminum (Al) and Europium (Eu) as cathode buffer layer (CBL). The ZnO:Al,Eu nanoparticle layer has broadband absorption in the ultraviolet (300-400 nm) region. The Al doping contributes to the enhancement in the conductivity whereas Eu doping significantly improves emission in the visible region. Moreover, this emission overlaps with the absorption range of polymer poly [N -9′-heptadecanyl-2,7-carbazole-alt-5,5-(4′,7′-di-2-thienyl-2′,1′,3′- benzothiadiazole)] (PCDTBT) significantly and results in an enhanced absorption by the active layer and hence high photocurrent. An increase in the power conversion efficiency (PCE) of 6.8% has been obtained for ZnO: Al,Eu CBL as compared to 5.9% for pristine ZnO, in the inverted device configuration ITO/CBL/active layer/MoOx/Al. The active layer comprises of a blend of PCDTBT donor and [6-6]-phenyl C71 butyric acid methyl ester (PC71BM) acceptor. In the reference device pristine ZnO has been used as CBL, whereas in the other one ZnO:Al,Eu has been used as CBL. The role of the luminescent CBL layer is to down-shift the UV light into visible range which overlaps with the absorption of PCDTBT polymer, resulting in an energy transfer from ZnO:Al,Eu to PCDTBT polymer and the absorption by active layer is enhanced as revealed by transient spectroscopy. This enhancement resulted in an increase in the short circuit current which contributes in an increased PCE in the device employing ZnO: Al,Eu CBL. Thus, the luminescent ZnO: Al, Eu nanoparticle CBL has great potential in organic solar cells.

Keywords: cathode buffer layer, energy transfer, organic solar cell, power conversion efficiency

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Authors: James Sinclair, Katy Soapi, Brad Carte

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The marine environment has continuously demonstrated to be a rich source of secondary metabolites and bioactive compounds that can address the many pharmaceutical problems facing mankind. The emergence of multidrug resistant pathogens has caused scientists to explore contemporary ways of combating these super bugs. A red-pigmented bacterial strain isolated from a marine alga collected in Fiji was identified to be Pseudoalteromonas rubra from 16s rRNA sequencing. This bacterial strain was cultured using a yeast-peptone media and incubated for five days. The ethyl acetate extract of this bacterium was subjected to chromatographic separation techniques such as vacuum liquid chromatography, flash chromatography, size exclusion chromatography and high-pressure liquid chromatography to yield the pure compound and a number of semi-pure fractions. The crude extract and subsequent purified fractions were analyzed by ultraviolet/visible spectroscopy and mass spectroscopy and was found to contain the compounds ivermectin, stenothricin, cyclo-L-pro-L-val, prodigiosin, mycophenolic acid, phenazine-1-carboxylic acid, eplerenone, staurosporine and pseudoalteromone A. The structure of the pure compound, pseudoalteromone A, was elucidated using NMR 1H, 13C, 1H-1H COSY, HSQC and HMBC spectroscopic data.

Keywords: Pseudoalteromonas rubra, Pseudoalteromone A, secondary metabolites, structure elucidation

Procedia PDF Downloads 177

Authors: S. A. Jumare, A. O. Tijani, M. F. Siraj, B. V. Babatunde

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This research investigated the comparative analysis of oil extracted from cotton and watermelon seeds using solvent extraction process. Normal ethyl-ether was used as solvent in the extraction process. The AOAC method of Analysis was employed in the determination of the physiochemical properties of the oil. The chemical properties of the oil determined include the saponification value, free fatty acid, iodine value, peroxide value and acid value. The physical properties of the oil determined include specific gravity, refractive index, colour, odour, taste and pH. The value obtained for cottonseed oil are saponification value (187mgKOH/g), free fatty acid (5.64mgKOH/g), iodine value (95.2g/100), peroxide value (9.33meq/kg), acid value (11.22mg/KOH/g), pH value (4.62), refractive index (1.46), and specific gravity (0.9) respectively, it has a bland odour, a reddish brown colour and a mild taste. The values obtained for watermelon seed oil are saponification value (83.3mgKOH/g), free fatty acid (6.58mg/KOH/g), iodine value (122.6g/100), peroxide value (5.3meq/kg), acid value (3.74mgKOH/g), pH value (6.3), refractive index (1.47), and specific gravity (0.9) respectively, it has a nutty flavour, a golden yellow colour and a mild taste. From the result obtained, it shows that cottonseed oil has high acid value which shows the stability of the oil and its stability to rancidity. Consequently, watermelon seed oil is order wise.

Keywords: extraction, solvent, cotton seeds, watermelon seeds

Procedia PDF Downloads 325

Authors: Komal Kumar, Sreedevi Upadhyayula

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In this study, a two-stage process was established for the synthesis of HMF esters using ionic liquid acid catalyst. Ionic liquid catalyst with different strength of the Bronsted acidity was prepared in the laboratory and characterized using 1H NMR, FT-IR, and 13C NMR spectroscopy. Solid acid catalyst from the ionic liquid catalyst was prepared using the immobilization method. The acidity of the synthesized acid catalyst was measured using Hammett function and titration method. Catalytic performance was evaluated for the biomass conversion to 5-hydroxymethylfurfural (5-HMF) and levulinic acid (LA) in methyl isobutyl ketone (MIBK)-water biphasic system. A good yield of 5-HMF and LA was found at the different composition of MIBK: Water. In the case of MIBK: Water ratio 10:1, good yield of 5-HMF was observed at ambient temperature 150˚C. Upgrading of 5-HMF into monoesters from the reaction of 5-HMF and reactants using biomass-derived monoacid were performed. Ionic liquid catalyst with -SO₃H functional group was found to be best efficient in comparative of a solid acid catalyst for the esterification reaction and biomass conversion. A good yield of 5-HMF esters with high 5-HMF conversion was found to be at 105˚C using the best active catalyst. In this process, process A was the hydrothermal conversion of cellulose and monomer into 5-HMF and LA using acid catalyst. And the process B was the esterification followed by using similar acid catalyst. All monoesters of 5-HMF synthesized here can be used in chemical, cross linker for adhesive or coatings and pharmaceutical industry. A theoretical density functional theory (DFT) study for the optimization of the ionic liquid structure was performed using the Gaussian 09 program to find out the minimum energy configuration of ionic liquid catalyst.

Keywords: biomass conversion, 5-HMF, Ionic liquid, HMF ester

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Authors: Ester Ato, Maria Angeles Fernández-Vilar, Maria Dolores Galián

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The aim of this work was to analyze the relation between children´s effortful control, marital adjustment and parenting practices in a sample of 345 Spanish children aged between 6 and 8 years. Traditionally, the literature confirms that a higher level of marital conflict has been associated with less effective and less positive parenting, but there are few studies that include the effect that children´s effortful control exert to this relation. To measure marital adjustment, parenting practices and children’s temperament, parents were given the Marital Adjustment Test (MAT), the Spanish version of the PCRI (Parent-Child Relationship Inventory), and the TMCQ (Temperament in Middle Childhood Questionnaire). The results confirmed that higher marital satisfaction predicted more positive parenting practices, whereas lower marital adjustment scores predicted less parenting support and control. Using a statistical modeling approach, we tested a moderation model that revealed the moderating role of effortful control in the relation between marital adjustment and parenting. Concretely, higher marital satisfaction predicts higher parenting communication and involvement, but only in children with low levels of effortful control. Therefore, a difficult temperament interferes in a less negative way in the family system when parents are satisfied and united. And a better self-regulated child predicts more effective parenting practice regardless of the parents´ marital satisfaction. The clinical implications of the present findings should be considered. Specifically, difficult children must be detected and evaluated in community settings, such as school or community programs, in order to take into account the marital adjustment and parenting practices of their parents, and to be able to design adequate family interventions and prevent future pathologizing patterns.

Keywords: effortful control, marital adjustment, parenting, moderation

Procedia PDF Downloads 382

Authors: Radovan Cobanovic, Milica Rankov Sicar

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Biodiesel refers to a vegetable oil - or animal fat-based diesel fuel consisting of long-chain alkyl (methyl, ethyl, or propyl) esters. It is derived by alcoholysis of triacylglycerols (triglycerides) from various lipid based materials that can be traditionally categorized into the following main groups: vegetable oils, animal fats, waste and algal oils. The goal of this study was to evaluate microbiological stability of biodiesel samples since it has been made from vegetable oil or animal fat which was stored on room temperature. For the purposes of this study, analyzes were conducted on six samples of biodiesel first at zero sample at the reception day than fifth, thirtieth, sixtieth, ninetieth and one hundred twentieth day from the day of reception. During this period, biodiesel samples were subjected to microbiological analyses (Salmonella spp., Listeria monocytogenes, Enterobacteriaceae and total plate count). All analyses were tested according to ISO methodology: Salmonella spp ISO 6579, Listeria monocytogenes ISO 11290-2, Enterobacteriaceae ISO 21528-1, total plate count ISO 4833-1. The results obtained after the analyses which were done according to the plan during the 120 days indicate that are no changes of products concerning microbiological analyses. Salmonella spp., Listeria monocytogenes, Enterobacteriaceae were not detected and results for total plate count showed values < 10 cfu/g for all six samples. On the basis of this monitoring under defined storage conditions at room temperatures, the results showed that biodiesel is very stable as far as microbiological analysis were concerned.

Keywords: biodiesel, microbiology, room temperature, stability

Procedia PDF Downloads 256