Search results for: ethylene methyl acrylate

Authors: Mazouzi Nourdjihane, K. Boutemak, A. Haddad, Y. Chegreouche

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In the last decades, biodegradable polymers have been considered as one of the most popular options for the delivery of drugs and various conventional doses. The film forming system (FFS) can be used in topical, transdermal, ophthalmic, oral and gastric applications. Recently this system has focused on improving drug delivery, which can promote drug release. In this context, the aim of this study is to create polymeric film-forming systems for the stomach and to evaluate and test their gastroprotective effects, comparing the effects of changes in composition on film characteristics. It uses a plant-derived polyphenol extract extracted from fennel to demonstrate anti-inflammatory activity in the film. The films are made from hydroxypropyl methylcellulose polymer and different types of plastic, glycerol and polyethylene glycol. The ffs properties show that MgO-glycerol-reinforced hydroxypropylmethylcellulose (HPMC-MgO-Gly) is better than that based on MgO-PEG-reinforced hydroxypropylmethylcellulose (HPMC-MgO-PEG). It is durable, has a faster drying time and allows for maximum recovery. Water vapor strength and blowing speed and other additions show another advantage of HPMC-MgO-Gly compared to HPMC-MgO-PEG, indicating good adhesion between the support (top) and film production. In this study, the gastroprotective effect of fennel phenol extract was found, showing that this plant material has a gastroprotective effect on ulcers and that the film can absorb the active substance.

Keywords: film formin system, hydroxypropyl methylcellulose, magnesium oxide, in vivo

Procedia PDF Downloads 53

Authors: T. S. Soliman, A. G. Galyas, E. V. Rusinova, S. A. Vshivkov

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The liquid crystals combining properties of a liquid and an anisotropic crystal substance play an important role in a science and engineering. Molecules of cellulose and its derivatives have rigid helical conformation, stabilized by intramolecular hydrogen bonds. Therefore the macromolecules of these polymers are capable to be ordered at dissolution and form liquid crystals of cholesteric type. Phase diagrams of solutions of some cellulose derivatives are known. However, little is known about the effect of a magnetic field on the viscosity of polymer solutions. The systems hydroxypropyl cellulose (HPC) – ethanol, HPC – ethylene glycol, HPC–DМАA, HPC–DMF, ethyl cellulose (EC)–ethanol, EC–DMF, were studied in the presence and absence of magnetic field. The solution viscosity was determined on a Rheotest RN 4.1 rheometer. The effect of a magnetic field on the solution properties was studied with the use of two magnets, which induces a magnetic-field-lines directed perpendicularly and parallel to the rotational axis of a rotor. Application of the magnetic field is shown to be accompanied by an increase in the additional assembly of macromolecules, as is evident from a gain in the radii of light scattering particles. In the presence of a magnetic field, the long chains of macromolecules are oriented in parallel with field lines. Such an orientation is associated with the molecular diamagnetic anisotropy of macromolecules. As a result, supramolecular particles are formed, especially in the vicinity of the region of liquid crystalline phase transition. The magnetic field leads to the increase in viscosity of solutions. The results were used to plot the concentration dependence of η/η0, where η and η0 are the viscosities of solutions in the presence and absence of a magnetic field, respectively. In this case, the values of viscosity corresponding to low shear rates were chosen because the concentration dependence of viscosity at low shear rates is typical for anisotropic systems. In the investigated composition range, the values of η/η0 are described by a curve with a maximum.

Keywords: rheology, liquid crystals, magnetic field, cellulose ethers

Procedia PDF Downloads 334

Authors: Qi Liu, Jiqin Yao, Xiaohu Zhou, Bo Zheng

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The first artificial cell was produced by Thomas Chang in the 1950s when he was trying to make a mimic of red blood cells. Since then, many different types of artificial cells have been constructed from one of the two approaches: a so-called bottom-up approach, which aims to create a cell from scratch, and a top-down approach, in which genes are sequentially knocked out from organisms until only the minimal genome required for sustaining life remains. In this project, bottom-up approach was used to build a new cell-free expression system which mimics artificial cell that capable of protein expression and communicate with each other. The artificial cells constructed from the bottom-up approach are usually lipid vesicles, polymersomes, hydrogels or aqueous droplets containing the nucleic acids and transcription-translation machinery. However, lipid vesicles based artificial cells capable of communication present several issues in the cell communication research: (1) The lipid vesicles normally lose the important functions such as protein expression within a few hours. (2) The lipid membrane allows the permeation of only small molecules and limits the types of molecules that can be sensed and released to the surrounding environment for chemical communication; (3) The lipid vesicles are prone to rupture due to the imbalance of the osmotic pressure. To address these issues, the hydrogel-based artificial cells were constructed in this work. To construct the artificial cell, polyacrylamide hydrogel was functionalized with Acrylate PEG Succinimidyl Carboxymethyl Ester (ACLT-PEG2000-SCM) moiety on the polymer backbone. The proteinaceous factors can then be immobilized on the polymer backbone by the reaction between primary amines of proteins and N-hydroxysuccinimide esters (NHS esters) of ACLT-PEG2000-SCM, the plasmid template and ribosome were encapsulated inside the hydrogel particles. Because the artificial cell could continuously express protein with the supply of nutrients and energy, the artificial cell-artificial cell communication and artificial cell-natural cell communication could be achieved by combining the artificial cell vector with designed plasmids. The plasmids were designed referring to the quorum sensing (QS) system of bacteria, which largely relied on cognate acyl-homoserine lactone (AHL) / transcription pairs. In one communication pair, “sender” is the artificial cell or natural cell that can produce AHL signal molecule by synthesizing the corresponding signal synthase that catalyzed the conversion of S-adenosyl-L-methionine (SAM) into AHL, while the “receiver” is the artificial cell or natural cell that can sense the quorum sensing signaling molecule form “sender” and in turn express the gene of interest. In the experiment, GFP was first immobilized inside the hydrogel particle to prove that the functionalized hydrogel particles could be used for protein binding. After that, the successful communication between artificial cell-artificial cell and artificial cell-natural cell was demonstrated, the successful signal between artificial cell-artificial cell or artificial cell-natural cell could be observed by recording the fluorescence signal increase. The hydrogel-based artificial cell designed in this work can help to study the complex communication system in bacteria, it can also be further developed for therapeutic applications.

Keywords: artificial cell, cell-free system, gene circuit, synthetic biology

Procedia PDF Downloads 130

Authors: Szymon Kugler, Krzysztof Kowalczyk, Tadeusz Spychaj

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An addition of carbon nanotubes (CNT) can simultaneously improve many features of epoxy coatings, i.e. electrical, mechanical, functional and thermal. Unfortunately, this nanofiller negatively affects visual properties of the coatings, such as transparency and gloss. The main reason for the low visual performance of CNT-modified epoxy coatings is the lack of compatibility between CNT and popular amine curing agents, although epoxy resins based on bisphenol A are indisputable good CNT dispersants. This is a serious obstacle in utilization of the coatings in advanced applications, demanding both high transparency and electrical conductivity. The aim of performed investigations was to find amine curing agents exhibiting affinity for CNT, and ensuring good performance of epoxy coatings with them. Commercially available CNT was dispersed in epoxy resin, as well as in different aliphatic, cycloaliphatic and aromatic amines, using one of two dispergation methods: ultrasonic or mechanical. The CNT dispersions were subsequently used in the preparation of epoxy coating compositions and coatings on a transparent substrate. It was found that amine derivative of bio-based cardanol, as well as modified o-tolylbiguanide exhibit significant CNT, dispersing properties, resulting in improved transparent/electroconductive performance of epoxy coatings. In one of prepared coating systems just 0.025 wt.% (250 ppm) of CNT was enough to obtain coatings with semi conductive properties, 83% of transparency as well as perfect chemical resistance to methyl-ethyl ketone and improved thermal stability. Additionally, a theory of the influence of amine chemical structure on CNT dispersing properties was proposed.

Keywords: bio-based cardanol, carbon nanotubes, epoxy coatings, tolylbiguanide

Procedia PDF Downloads 189

Authors: Souhir Abid

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The growing interest in vegetal biomass as an alternative for fossil resources has stimulated the development of numerous classes of monomers. Polymers from renewable resources have attracted an increasing amount of attention over the last two decades, predominantly due to two major reasons (i) firstly environmental concerns, and (ii) secondly the use of monomers from renewable feedstock is a steadily growing field of interest in order to reduce the amount of petroleum consumed in the chemical industry and to open new high-value-added markets to agriculture. Furanic polymers have been considered as alternative environmentally friendly polymers. In our earlier work, modifying furanic polyesters by incorporation of amide functions along their backbone, lead to a particular class of polymer ‘poly(ester-amide)s’, was investigated to combine the excellent mechanical properties of polyamides and the biodegradability of polyesters. As a continuation of our studies on this family of polymer, a series of furanic poly(ester-amide)s bearing sulfonate groups in the main chain were synthesized from 5,5’-Isopropylidene-bis(ethyl 2-furoate), dimethyl 5-sodiosulfoisophthalate, ethylene glycol and hexamethylene diamine by melt polycondensation using zinc acetate as a catalyst. In view of the complexity of the NMR spectrum analysis of the resulting sulfonated poly(ester-amide)s, we found that it is useful to prepare initially the corresponding homopolymers: sulfonated polyesters and polyamides. Structural data of these polymers will be used as a basic element in 1H NMR characterization. The hydrolytic degradation in acidic aqueous conditions (pH = 4,35 ) at 37 °C over the period of four weeks show that the mechanism of the hydrolysis of poly(ester amide)s was elucidated in relation with the microstructure. The strong intermolecular hydrogen bonding interactions between amide functions and water molecules increases the hydrophilicity of the macromolecular chains and consequently their hydrolytic degradation.

Keywords: furan, hydrolytic degradation, polycondensation, poly(ester amide)

Procedia PDF Downloads 275

Authors: Nabila Berrighi, Kaddour Bouderoua, Maria Khossif, Gema Nieto, Gaspar Ros

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Ruminant meat is an important source of nutrients and is also of high sensory value. However, the importance and nature of these characteristics depend on ruminant nutrition. The objective of this study is to assess the effect of two Algerian feeding systems applied in the steppic rearing area of Djelfa and in the highlands one of Tiaret on the growth performance of lambs and on their meat quality, especially on their aroma compounds of meat. At the beginning of the experiment, lambs had an average body weight of 34.04 kg, and 35.40 kg for the group reared at Highland (0% concentrate) and Steppe (30% concentrate), respectively. The incorporation of the concentrated feed in Steppe had a significant effect on slaughter weight compared to lambs fed only on pasture (Highland) (49.72 Kg vs. 42.06 Kg, P<0.05). Beyond the first month, animals from the Steppe one showed better weight gains compared to those from Highland (14.32Kg vs. 8.02 Kg, respectively, P<0,05). After slaughter, samples from the Longissimus thoracis were removed and analyzed. The results point to significant differences in the amounts of many of the predominant volatile compounds between both groups (p<0.05), such as Hexanal, 2-methyl-3-furanthiol and nonanal (8.92 μg/kg vs. 4.57 μg/kg), (8.88 μg/kg vs. 7.45 μg/kg) and (2.09 μ/kg vs. 1.02 μg/kg) associated with smells of green, boiling meat and orange fruit, respectively. These compounds, measured by olfactometry, derived from the oxidation of lipids and appear to be responsible for the characteristic flavor of lamb meat in the steppe compared to that generated by meat from animals from the Highland pastures. The Algerian Steppe ecosystem is very interesting for outdoor sheep breeding, which allows to obtain attractive sensory quality and in the production of typical lamb meat that can be considered as a label.

Keywords: falvour, growth performance, lamb meat, steppe pasture

Procedia PDF Downloads 72

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

Procedia PDF Downloads 183

Authors: K. Drabczyk, Z. Starowicz, S. Maleczek, P. Zieba

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The army, police and fire brigade commonly use dedicated equipment based on special textile materials. The properties of these textiles should ensure human life and health protection. Equally important is the ability to use electronic equipment and this requires access to the source of electricity. Photovoltaic cells integrated with such textiles can be solution for this problem in the most of outdoor circumstances. One idea may be to laminate the cells to textile without changing their properties. The main goal of this work was analyzed lamination quality of special designed semi-flexible solar module with special textile materials as a backsheet. In the first step of investigation, the quality of lamination was determined using device equipped with dynamometer. In this work, the crystalline silicon solar cells 50 x 50 mm and thin chemical tempered glass - 62 x 62 mm and 0.8 mm thick - were used. The obtained results showed the correlation between breaking force and type of textile weave and fiber. The breaking force was in the ranges: 4.5-5.5 N, 15-20 N and 30-33 N depending on the type of wave and fiber type. To verify these observations the microscopic and FTIR analysis of fibers was performed. The studies showed the special textile can be used as a backsheet of semi-flexible solar modules. This work presents a new composition of solar module with special textile layer which, to our best knowledge, has not been published so far. Moreover, the work presents original investigations on adhesion of EVA (ethylene-vinyl acetate) polymer to textile with respect to fiber structure of laminated substrate. This work is realized for the GEKON project (No. GEKON2/O4/268473/23/2016) sponsored by The National Centre for Research and Development and The National Fund for Environmental Protection and Water Management.

Keywords: flexible solar modules, lamination process, solar cells, textile for photovoltaics

Procedia PDF Downloads 345

Authors: Yesim Özogul, Fethiye Takadaş, Mustafa Durmus, Yılmaz Ucar, Ali Rıza Köşker, Gulsun Özyurt, Fatih Özogul

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It has been well documented that polyunsaturated fatty acids (PUFAs), especially eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) have beneficial effects on health, regarding prevention of cardiovascular diseases, cancer and autoimmune disorders, development the brain and retina and treatment of major depressive disorder etc. Thus, an adequate intake of omega PUFA is essential and generally marine fish are the richest sources of PUFA in human diet. Thus, this study was conducted to evaluate the efficiency of different extraction methods (Bligh and Dyer, soxhlet, microwave and ultrasonics) on the fat content and fatty acid profiles of marine fish species (Mullus babatus, Upeneus moluccensis, Mullus surmuletus, Anguilla anguilla, Pagellus erythrinus and Saurida undosquamis). Fish species were caught by trawl in Mediterranean Sea and immediately iced. After that, fish were transported to laboratory in ice and stored at -18oC in a freezer until the day of analyses. After extracting lipid from fish by different methods, lipid samples were converted to their constituent fatty acid methyl esters. The fatty acid composition was analysed by a GC Clarus 500 with an autosampler (Perkin Elmer, Shelton, CT, USA) equipped with a flame ionization detector and a fused silica capillary SGE column (30 m x 0.32 mm ID x 0.25 mm BP20 0.25 UM, USA). The results showed that there were significant differences (P < 0.05) in fatty acids of all species and also extraction methods affected fat contents and fatty acid profiles of fish species.

Keywords: extraction methods, fatty acids, marine fish, PUFA

Procedia PDF Downloads 246

Authors: Mahmoud A. Abdulhamid

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Poly(ether-ether-ketone) (PEEK) has received increased attention due to its outstanding performance in different membrane applications including gas and liquid separation. However, it suffers from a semi-crystalline morphology, bad solubility and low porosity. To fabricate membranes from PEEK, the usage of harsh acid such as sulfuric acid is essential, regardless its hazardous properties. In this work, we report the molecular design of poly(ether-ether-ketones) (iPEEKs) with intrinsic porosity character, by incorporating kinked units into PEEK backbone such as spirobisindane, Tröger's base, and triptycene. The porous polymers were used to fabricate stable membranes for organic solvent nanofiltration application. To better understand the mechanism, we conducted molecular dynamics simulations to evaluate the possible interactions between the polymers and the solvents. Notable enhancement in separation performance was observed confirming the importance of molecular engineering of high-performance polymers. The iPEEKs demonstrated good solubility in polar aprotic solvents, a high surface area of 205–250 m² g⁻¹, and excellent thermal stability. Mechanically flexible nanofiltration membranes were prepared from N-methyl-2-pyrrolidone dope solution at iPEEK concentrations of 19–35 wt%. The molecular weight cutoff of the membranes was fine-tuned in the range of 450–845 g mol⁻¹ displaying 2–6 fold higher permeance (3.57–11.09 L m⁻² h⁻¹ bar⁻¹) than previous reports. The long-term stabilities were demonstrated by a 7 day continuous cross-flow filtration.

Keywords: molecular engineering, polymer synthesis, membrane fabrication, liquid separation

Procedia PDF Downloads 82

Authors: Boda Sreenivas, Lyathakula Ravindranath, Kanugula Srishailam, Byru Venkatram Reddy

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Extensive research into the optimized structure and molecular properties of 3-Flouro-2-methylbenzoicacid(FMB), 3-Chloro-2-methoxybenzoicacid (CMB), and 3-Bromo-2-methylbenzoicacid (BMB) was carried out using FT-IR, FT-Raman and UV-Visible spectra, as well as theoretically using the DFT approach with B3LYPfunctional in conjunction with 6-311++G(d,p) basis set. The optimized structure was determined by evaluating torsional scans about free rotation bonds. Structure parameters, harmonic vibrational frequencies, potential energy distribution(PED), and infrared and Raman intensities were computed. The computational results from the DFT approach, such asFT-IR, FT-Raman, and UV-Visible spectra, were compared with the experimental results and found good agreement. Observed and calculated frequencies agreed with an rms error of 8.42, 6.60, and 6.95 cm-1 for FMB, CMB, and BMB, respectively. Unambiguous vibrational assignments were made for all fundamentals using PED and eigenvectors. The electronic HOMO-LUMO, H-bonding, and strong conjugative interactions across different molecular entities are discussed using experimental and simulated Ultraviolet-Visible spectra. The title molecules' molecular properties such as dipole moment, mean polarizability, and first-order hyperpolarizability, were calculated to study their non-linear optical (NLO) behavior. The chemical reactivity descriptors and mapped electrostatic surface potential (MESP) were also evaluated. Natural bond orbital (NBO) analysis was used to examine the stability of molecules resulting from hyperconjugative interactions and charge delocalization.

Keywords: ftir/raman spectra, DFT, NLO, homo-lumo, NBO, halogenated benzoic acids

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Authors: Jaime Pizarro, Ximena Castillo

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The intensive use of water in agriculture, industry, human consumption and increasing pollution are factors that reduce the availability of water for future generations; the challenge is to advance in sustainable and low-cost solutions to reuse water and to facilitate the availability of the resource in quality and quantity. The use of new low-cost materials with sorbent capacity for pollutants is a solution that contributes to the improvement and expansion of water treatment and reuse systems. Fly ash, a residue from the combustion of coal in power plants that is produced in large quantities in newly industrialized countries, contains a high amount of silicon oxides and aluminum oxides, whose properties can be used for the synthesis of mesoporous materials. Properly functionalized, this material allows obtaining matrixes with high sorption capacity. The mesoporous materials have a large surface area, thermal and mechanical stability, uniform porous structure, and high sorption and functionalization capacities. The goal of this study was to develop hexagonal mesoporous siliceous material (HMS) for the adsorption of sulphate from industrial and mining waters. The silica was extracted from fly ash after calcination at 850 ° C, followed by the addition of water. The mesoporous structure has a surface area of 282 m2 g-1 and a size of 5.7 nm and was functionalized with ethylene diamine through of a self-assembly method. The material was characterized by Diffuse Reflectance Infrared Fourier Transform Spectroscopy (DRIFTS). The capacity of sulphate sorption was evaluated according to pH, maximum load capacity and contact time. The sulphate maximum adsorption capacity was 146.1 mg g-1, which is three times higher than commercial sorbents. The kinetic data were fitted according to a pseudo-second order model with a high coefficient of linear regression at different initial concentrations. The adsorption isotherm that best fitted the experimental data was the Freundlich model.

Keywords: fly ash, mesoporous siliceous, sorption, sulphate

Procedia PDF Downloads 140

Authors: R. F. Vieira, S. A. Figueiredo, O. M. Freitas, V. F. Domingues, C. Delerue-Matos

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The presence of sulphur compounds like hydrogen sulphide and mercaptans is one of the reasons for waste-water treatment and waste management being associated with odour emissions. In this context having a quantifying method for these compounds helps in the optimization of treatment with the goal of their elimination, namely biofiltration processes. The aim of this study was the development of a method for quantification of odorous gases in waste treatment plants air samples. A method based on head space solid phase microextraction (HS-SPME) coupled with gas chromatography - flame photometric detector (GC-FPD) was used to analyse H2S and Metil Mercaptan (MM). The extraction was carried out with a 75-μm Carboxen-polydimethylsiloxane fiber coating at 22 ºC for 20 min, and analysed by a GC 2010 Plus A from Shimadzu with a sulphur filter detector: splitless mode (0.3 min), the column temperature program was from 60 ºC, increased by 15 ºC/min to 100 ºC (2 min). The injector temperature was held at 250 ºC, and the detector at 260 ºC. For calibration curve a gas diluter equipment (digital Hovagas G2 - Multi Component Gas Mixer) was used to do the standards. This unit had two input connections, one for a stream of the dilute gas and another for a stream of nitrogen and an output connected to a glass bulb. A 40 ppm H2S and a 50 ppm MM cylinders were used. The equipment was programmed to the selected concentration, and it automatically carried out the dilution to the glass bulb. The mixture was left flowing through the glass bulb for 5 min and then the extremities were closed. This method allowed the calibration between 1-20 ppm for H2S and 0.02-0.1 ppm and 1-3.5 ppm for MM. Several quantifications of air samples from inlet and outlet of a biofilter operating in a waste management facility in the north of Portugal allowed the evaluation the biofilters performance.

Keywords: biofiltration, hydrogen sulphide, mercaptans, quantification

Procedia PDF Downloads 457

Authors: Wassim Guermazi, Saoussan Boukhris, Neila Annabi Trabelsi, Tarek Rebai, Alya Sellami-Kamoun, Habib Ayadi

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This work investigates the protective effects of the microalga Halamphora sp. extract (H. Ext) as a natural product on lead-intoxicated liver and kidney human cells in vitro and in vivo on rats wistar. HepG2 cells line derived from human hepatocellular carcinoma and HEK293 cells line derived from human embryonic kidney were used for the in vitro study. The analysis of the fatty acids methyl esters of the extract was performed by a GC/MS. Four groups of rats, each of which was composed of six animals, were used for the in vivo experiment. The pretreatment of HepG2 and HEK293 cells line with the extract (100 µg mL-1) significantly (p < 0.05) protected against cytotoxicity induced by lead exposure. In vivo, the biochemical parameters in serum, namely malondialdehyde level (MDA), superoxide dismutase (SOD), catalase (CAT) and glutathione peroxidase (GPx) activities, were measured in supernatants of organ homogenates. H. Ext was found to be rich in fatty acids, essentially palmitic and palmitoleic accounting respectively 29.46% and 42.07% of total fatty acids. Both in vitro and in vivo, the co-treatment with H. Ext allowed the protection of the liver and kidney cells structure, as well as the significant preservation of normal antioxidant and biochemical parameters in rats. Halamphora extract rich in fatty acids has been proven to be effective in protection against Pb-induced toxicity.

Keywords: microalga extract, human cells line, fatty acid, lead exposure, oxidative stress, rats

Procedia PDF Downloads 66

Authors: Shubham Sharma, Sandra Barkauskaite, Brendan Duffy, Swarna Jaiswal, Amit K. Jaiswal

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Food packaging protects food from temperature, light, and humidity; preserves food and guarantees the safety and the integrity of the food. Advancement in packaging research leads to development of active packaging system with numerous properties such as oxygen scavengers, carbon-dioxide generating systems, antimicrobial active packaging, moisture control packaging, ethylene scavengers etc. In the active packaging, several additives such as essential oils, polyphenols etc. are incorporated into packaging film or within the packaging material to achieve the desired properties. This study investigates the effect on the structural, thermal and functional properties of different poly(lactide) – poly (butylene adipate-co-terephthalate) (PLA-PBAT) blend films incorporated with clove essential oil. The PLA-PBAT films were prepared by a solution casting method and then characterized based on their optical, mechanical properties, surface hydrophobicity, chemical composition, antimicrobial activity against S. aureus and E. coli, and inhibition of biofilm formation of E. coli. Results showed that, the developed packaging film containing clove oil has significant UV-blocking property (80%). However, incorporation of clove oil resulted in reduced transparency and tensile strength of the film as the concentration of clove oil increased. The surface hydrophobicity of packaging film was improved with the increasing concentration of essential oil. Similarly, thickness of the clove oil containing films increased from 36.71 µm to 106.67 µm as the concentration increases. The antimicrobial activity and biofilm inhibition study showed that the clove-incorporated PLA-PBAT composite film was effective against tested bacteria E. coli and S. aureus. This study showed that the PLA-PBAT – Clove oil composite film has significant antimicrobial and UV-blocking properties and can be used as an active food packaging film.

Keywords: active packaging, clove oil, poly(butylene adipate-co-terephthalate), poly(lactide)

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Authors: Fabio T. Costa, Sergio E. Moya, Marcelo H. Sousa

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Nanocomposites designed by embedding magnetic nanoparticles into a polymeric matrix stand out as ideal magnetic-hybrid and magneto-responsive materials as sorbents for removal of pollutants in environmental applications. Covalent coupling is often desired for the immobilization of species on these nanocomposites, in order to keep them permanently bounded, not desorbing or leaching over time. Moreover, unwanted adsorbates can be separated by successive washes/magnetic separations, and it is also possible to recover the adsorbate covalently bound to the nanocomposite surface through detaching/cleavage protocols. Thus, in this work, we describe the preparation and characterization of highly-magnetizable chloromethylated polystyrene-based nanocomposite beads for selective covalent coupling in environmental applications. For synthesis optimization, acid resistant core-shelled maghemite (γ-Fe₂O₃) nanoparticles were coated with oleate molecules and directly incorporated into the organic medium during a suspension polymerization process. Moreover, the cross-linking agent ethylene glycol dimethacrylate (EGDMA) was utilized for co-polymerization with the 4-vinyl benzyl chloride (VBC) to increase the resistance of microbeads against leaching. After characterizing samples with XRD, ICP-OES, TGA, optical, SEM and TEM microscopes, a magnetic composite consisting of ~500 nm-sized cross-linked polymeric microspheres embedding ~8 nm γ-Fe₂O₃ nanoparticles was verified. This nanocomposite showed large room temperature magnetization (~24 emu/g) due to the high content in maghemite (~45 wt%) and resistance against leaching even in acidic media. Moreover, the presence of superficial chloromethyl groups, probed by FTIR and XPS spectroscopies and confirmed by an amination test can selectively adsorb molecules through the covalent coupling and be used in molecular separations as shown for the selective removal of 4-aminobenzoic acid from a mixture with benzoic acid.

Keywords: nanocomposite, magnetic nanoparticle, covalent separation, pollutant removal

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Authors: Edwin O. Clarke, Akintade O. Adeboyejo

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Intensive use of pesticides resulted in dispersal of pollutants throughout the globe. This study was carried out to investigate persistent Organochlorine pesticides (POPs) in water, sediment and fin fishes, Schilbes mystus and Hemichromis fasciatus from two different sampling stations along River Ogun between the month of June 2012 and January 2013. The Organochlorine pesticides analyzed include DDT (pp’1,1,1-trichloro-2,2-bis-(4-chlorophenyl) ethane), DDD, DDE (pp1,1-dichloro-2, 2-bis-(4-chlorophenyl) ethylene, HCH (gamma 1,2,3,4,5,6-hexachlorocylohexane, HCB hexachlorobenzene),Dieldrin (1,2,3,4,10,10-hexachloro-6,7-epoxy-1,4,4a,5,6,7,8,8a octahydro- 1,4,5,8 dimethanonaphthalene). The analysis was done using Gas Chromatograph with Electron Capture Detector. In water sample, the result showed that PPDDT, Endrin aldehyde, Endrin ketone concentrations were high in both stations. The mean value of Organochlorine analyzed in water range from Beta BHC (0.50±0.10µg/l) to PP DDT (162.86±0.21µg/l) in Kara sample station and Beta BHC (0.20±0.07µg/l) to Endrin Aldehyde (76.47±0.02µg/l) in Odo-Ogun sample station. The levels of POPs obtained in sediments ranged from 0.40±0.23µg/g (Beta BHC) to 259.90 ± 1.00µg/kg (Endosulfan sulfate) in Kara sample station and 0.64±0.00µg/g (Beta BHC) to 379.77 ±0.15 µg/g (Endosulfan sulfate) in Odo-Ogun sample station. The levels of POPs obtained in fin fish samples ranged from 0.29±0.00µg/g (Delta BHC) to 197.87 ± 0.31µg/g (PP DDT) in Kara sample station and in Odo-Ogun sample station the mean value for fish samples range from 0.29 ± 0.00 µg/g (Delta BHC) to 197.87 ± 0.32 µg/g (PP DDT). The study showed that the accumulation of POPs affect the environment and reduce water quality. The results showed that the concentrations were found to exceed the maximum acceptable concentration of 0.10µg/l value set by the European Union for the protection of freshwater aquatic life and this can be hazardous if the trend is not checked.

Keywords: hazardous, persistent, pesticides, biomes

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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: Howaida I. Abd-Alla, Nagwa M. M. Shalaby

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The fruit rind of Fortunella margarita (Nagami Kumkuat) was investigated for its chemical constituents. Thirteen metabolites were obtained and classified into, a sterol; β-sitosterol (1) and twelve phenolic compounds, three coumarins; xanthotoxin (2), isopimpinellin (3), umbelliferone (4), nine flavonoids of O-glycosides of flavone; apigenin-7-O-β-D-glucopyranoside (5), apigenin-7-O-rhamnoglucoside (rhoifolin) (6), C-glycosides; vitexin (7), vicenin II (8), and the methoxylated; 6-methoxyapigenin-7-methyl ether (9) and tangeretin (10) as well as flavanones class; naringenin (11), liquiritigenin (12), hesperdin (hesperetin-7-rhamnoglucoside) (13). All compounds were identified for the first time in F. margarita except compound (8). The major glycosides 5, 6, and 13 and total crude extract showed potential antiviral activity against live Newcastle disease virus vaccine strains (Komarov and LaSota) and live infectious bursitis viruses vaccine strain D78 replication in VERO cell cultures and on specific pathogen-free embryonated chicken eggs. Antiviral inhibitory concentration fifty (IC50), cytotoxic concentration fifty (CC50), and therapeutic index (TI) were calculated. In addition, the extract and compounds 7 and 13 showed marked antimicrobial activity against different strains of fungi, Gram-positive and negative bacteria, including some foodborne pathogens of animal origin, caused human disease. These results suggested that the extract of F. margarita may be considered potentially useful as a source of natural antiviral and antimicrobial agents. It can be used as an ingredient for functional food and/or pharmaceuticals.

Keywords: antimicrobial, antiviral, Fortunella margarita, Nagami Kumkuat, phenolic secondary metabolites

Procedia PDF Downloads 186

Authors: Ismail Celik, Gulgun Ayhan Kilcigil, Berna Guven, Zumra Kara, Arzu Onay-Besikci

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Epidermal Growth Factor Receptor is the cell-surface receptor of the ErbB (erythroblastic leukemia viral oncogene homologue receptors) family of tyrosine kinases. It plays a vital role in regulating the proliferation and differentiation of cells. However, a variety of mechanisms, such as EGFR expression, mutation, and ligand-dependent receptor dimerization, are associated with the development of various activated EGFR tumors. EGFR is highly expressed in most solid tumors, including breast, head and neck cancer, non-small cell lung cancer (NSCLC), renal, ovarian, and colon cancers. Thus, specific EGFR inhibition plays one of the key roles in cancer treatment. The compounds used in the treatment as tyrosine kinase inhibitors are known to contain the benzimidazole isosterium indole, pazopanib, and axitinibin indazole rings. In addition, benzimidazoles have been shown to exhibit protein kinase inhibitory activity in addition to their different biological activities.Based on these data, it was planned and synthesized of some oxadiazole bearing benzimidazole derivatives [N-cyclohexyl-5-((2-phenyl/substitutedphenyl-1H-benzo[d]imidazole-1-yl) methyl)-1,3,4-oxadiazole-2-amine]. EGFR kinase inhibitory efficiency of the synthesized compounds was determined by comparing them with a known kinase inhibitor erlotinib in vitro, and two of the compounds bearing phenyl (19a) and 3,4-dibenzyloxyphenyl (21a) ring exhibited significant activities.

Keywords: benzimidazole, EGFR kinase inhibitory, oxadiazole, synthesis

Procedia PDF Downloads 118

Authors: S. Jaramillo, Y. Montoya, W. Agudelo, J. Bustamante

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Cardiovascular diseases (CVD) are related to affectations of the heart and blood vessels, within these are pathologies such as coronary or peripheral heart disease, caused by the narrowing of the vessel wall (atherosclerosis), which is related to the accumulation of Low-Density Lipoproteins (LDL) in the arterial walls that leads to a progressive reduction of the lumen of the vessel and alterations in blood perfusion. Currently, the main therapeutic strategy for this type of alteration is drug treatment with statins, which inhibit the enzyme 3-hydroxy-3-methyl-glutaryl-CoA reductase (HMG-CoA reductase), responsible for modulating the rate of cholesterol production and other isoprenoids in the mevalonate pathway. This enzyme induces the expression of LDL receptors in the liver, increasing their number on the surface of liver cells, reducing the plasma concentration of cholesterol. On the other hand, when the blood vessel presents stenosis, a surgical procedure with vascular implants is indicated, which are used to restore circulation in the arterial or venous bed. Among the materials used for the development of vascular implants are Dacron® and Teflon®, which perform the function of re-waterproofing the circulatory circuit, but due to their low biocompatibility, they do not have the ability to promote remodeling and tissue regeneration processes. Based on this, the present research proposes the development of a hydrolyzed collagen and polyethylene oxide electrospun membrane reinforced with medium and high-intensity statins, so that in future research it can favor tissue remodeling processes from its microarchitecture.

Keywords: atherosclerosis, medium and high-intensity statins, microarchitecture, electrospun membrane

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Authors: Yusha'u Shu'aibu Baraya, Kah Keng Wong, Nik Soriani Yaacob

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Strobilanthes crispus (S. crispus), is a Malaysian herb locally known as ‘Pecah kaca’ or ‘Jin batu’ which have demonstrated potent anticancer effects in both in vitro and in vivo models. In particular, S. crispus subfraction (SCS) significantly reduced tumor growth in N-methyl-N-Nitrosourea-induced breast cancer rat model. However, there is paucity of information on the effects of SCS in breast cancer metastasis. Thus, in this study, the antimetastatic effects of SCS (100 mg/kg) was investigated following 30 days of treatment in 4T1-induced mammary tumor (n = 5) model. The response to treatment was assessed based on the outcome of the tumour growth, body weight and hematological parameters. The results demonstrated that tumor bearing mice treated with SCS (TM-S) had significant (p<0.05) reduction in the mean tumor number and tumor volume as well as tumor weight compared to the tumor bearing mice (TM), i.e. tumor untreated group. Also, there was no secondary tumor formation or tumor-associated lesions in the major organs of TM-S compared to the TM group. Similarly, comparable body weights were observed among the TM-S, normal (uninduced) mice treated with SCS and normal (untreated/control) mice (NM) groups compared to the TM group (p<0.05). Furthermore, SCS administration does not cause significant changes in the hematological parameters as compared to the NM group, which indicates no sign of anemia and toxicity related effects. In conclusion, SCS significantly inhibited the overall tumor growth and metastasis in 4T1-induced breast cancer mouse model suggesting its promising potentials as therapeutic agent for breast cancer treatment.

Keywords: 4T1-cells, breast cancer, metastasis, Strobilanthes crispus

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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: Ambreen Aslam, Tahira Aziz Mughal, Skye R. Thomas-Hall, Peer M. Schenk

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Biodiesel is an alternative to petroleum-derived fuel mainly composed of fatty acid from oleaginous microalgae feedstock. Microalgae produced fatty acid methyl esters (FAMEs) as they can store high levels of lipids without competing for food productivity. After lipid extraction and esterification, fatty acid profile from algae feedstock possessed the abundance of fatty acids with carbon chain length specifically C16 and C18. The qualitative analysis of FAME was done by cultivating mix microalgae consortia under three different CO₂ concentrations (1%, 3%, and 5.5%) from a coal fired flue gas. FAME content (280.3 µg/mL) and productivity (18.69 µg/mL/D) was higher under 1% CO₂ (flue gas) as compare to other treatments. Whereas, Mixed C. (F) supplemented with 5.5% CO₂ (50% flue gas) had higher SFA (36.28%) and UFA (63.72%) which improve the oxidative stability of biodiesel. Subsequently, low Iodine value (136.3 gI₂/100g) and higher Cetane number (52) of Mixed C.+P (F) were found to be in accordance with European (EN 14214) standard under 5.5% CO₂ along with 50mM phosphate buffer. Experimental results revealed that sufficient phosphate reduced FAME productivity but significantly enhance biodiesel quality. This research aimed to develop an integrated approach of utilizing flue gas (as CO₂ source) for significant improvement in biodiesel quality under surplus phosphorus. CO₂ sequestration from industrial flue gas not only reduce greenhouse gases (GHG) emissions but also ensure sustainability and eco-friendliness of the biodiesel production process through microalgae.

Keywords: biodiesel analysis, carbon dioxide, coal fired flue gas, FAME productivity, fatty acid profile, fuel properties, lipid content, mixed culture microalgae

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Authors: Rajani Kant Rai, Jayakrishnan Athipet

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There have been several attempts to prepare polymers with antimicrobial properties by doping with various N-halamines. Hydantoins (Cyclic N-halamine) is of importance due to their stability rechargeable chloroamide function, broad-spectrum anti-microbial action and ability to prevent resistance to the organisms. Polymerizable hydantoins are synthesized by tethering vinyl moieties to 5,5,-dialkyl hydantoin sacrificing the imide hydrogen in the molecule thereby restricting the halogen capture only to the amide nitrogen that results in compromised antibacterial activity. In order to increase the activity of the antimicrobial polymer, we have developed a scheme to maximize the attachment of chlorine to the amide and the imide moieties of hydantoin. Vinyl hydantoin monomer, (Z)-5-(4-((3-methylbuta-1,3-dien-2-yl)oxy)benzylidene)imidazolidine-2,4-dione (MBBID) was synthesized and copolymerized with a commercially available monomer, methyl methacrylate, by free radical polymerization. The antimicrobial activity of hydantoin is strongly dependent on their surface area and hence their microbial activity increases when incorporated in microspheres or nanoparticles as compared to their bulk counterpart. In this regard, smooth and rough surface microsphere of the vinyl monomer (MBBID) with commercial monomer was synthesized. The oxidative chlorine content of the copolymer ranged from 1.5 to 2.45 %. Further, to demonstrate the water purification potential, the thin column was packed with smooth or rough microspheres and challenged with simulated contaminated water that exhibited 6 log kill (total kill) of the bacteria in 20 minutes of exposure with smooth (25 mg/ml) and rough microsphere (15.0 mg/ml).

Keywords: cyclic N-halamine, vinyl hydantoin monomer, rough surface microsphere, simulated contaminated water

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Authors: El-Said I. El-Shafey, Syeda Naheed F. Ali, Saleh S. Al-Busafi, Haider A. J. Al-Lawati

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Date palm leaflets were utilized as a precursor for activated carbon (AC) preparation using KOH activation. AC produced was oxidized using nitric acid producing oxidized activated carbon (OAC). OAC that possesses acidic surface was surface functionalized to produce basic activated carbons using linear diamine compounds (ethylene diamine and propylene diamine). OAC was also functionalized to produce hydrophobic activated carbons using ethylamine (EA) and aniline (AN). Dehydrated carbon was also prepared from date palm leaflets using sulfuric acid dehydration/ oxidation and was surface functionalized in the same way as AC. Nitric acid oxidation was not necessary for DC as it is acidic carbon. The surface area of AC is high (823 m2/g) with microporosity domination, however, after oxidation and surface functionalization, both the surface area and surface microporosity decrease tremendously. DC surface area was low (15 m2/g) with mesoporosity domination. Surface functionalization has decreased the surface area of activated carbons. FTIR spectra show that -COOH group on DC and OAC almost disappeared after surface functionalization. The surface chemistry of all carbons produced was tested for pHzpc, basic sites, boehm titration, thermogravimetric analysis and zeta potential measurement. Scanning electron microscopy and energy dispersive spectroscopy in addition to CHN elemental analysis were also carried out. DC and OAC possess low pHzpc and high surface functionality, however, basic and hydrophobic carbons possess high pHzpc and low surface functionality. The different behavior of carbons is related to their different surface chemistry. Methylene blue adsorption was found to be faster on hydrophobic carbons based on AC and DC. The Larger adsorption capacity of methylene blue was found for hydrophobic carbons. Dominating adsorption forces of methylene blue varies from carbon to another depending on its surface nature. Sorption forces include hydrophobic forces, H-bonding, electrostatic interactions and van der Waals forces.

Keywords: carbon, acidic, basic, hydrophobic

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Authors: Syed Farooq Adil, Merajuddinkhan, Mujeeb Khan, Hamad Z. Alkhathlan

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Phytochemicals from plant extracts belong to an important source of natural products which have demonstrated excellent cytotoxic activities. However, plants of different origins exhibit diverse chemical compositions and bioactivities. Therefore, the discovery of plants based new anticancer agents from different parts of the world is always challenging. In this study, methanolic extracts of different parts of 11 plants from Saudi Arabia have been tested in vitro for their anticancer potential on human liver cancer cell line (HepG2). Particularly, for this study, plants from Asteraceae, Resedaceae, and Polygonaceae families were chosen on the basis of locally available ethnobotanical data and their medicinal properties. Among 12 tested extract samples, three samples obtained from Artemisia monosperma stem, Ochradenus baccatus aerial parts, and Pulicaria glutinosa stem have demonstrated interesting cytotoxic activities with a cell viability of 29.3%, 28.4% and 24.2%, respectively. Whereas, four plant extracts including Calendula arvensis aerial parts, Scorzonera musilii whole plant, A. monosperma leaves show moderate anticancer properties bearing a cell viability ranging from 11.9 to 16.7%. The remaining extracts have shown poor cytotoxic activities. Subsequently, GC-MS analysis of methanolic extracts of the four most active plants extracts such as C. comosum, O. baccatus, P. glutinosa and A. monosperma detected the presence of 41 phytomolecules. Among which 3-(4-hydroxyphenyl) propionitrile (1), 8,11-octadecadiynoic acid methyl ester (2), 6,7-dimethoxycoumarin (3), and 1-(2-hydroxyphenyl) ethenone (4) were found to be the lead compounds of C. comosum, O. baccatus P. glutinosa and A. monosperma, respectively.

Keywords: medicinal plants, asteraceae, polygonaceae, hepg2

Procedia PDF Downloads 111

Authors: Ç. Gökçek-Saraç, Ş. Özen, N. Derin

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The N-methyl-D-aspartate (NMDA)-dependent pathway is the major intracellular signaling pathway implemented in both short- and long-term memory formation in the hippocampus which is the most studied brain structure because of its well documented role in learning and memory. However, little is known about the effects of RF-EMR exposure on NMDA receptor signaling pathway including activation of protein kinases, notably Ca²⁺/calmodulin-dependent protein kinase II alpha (CaMKIIα). The aim of the present study was to investigate the effects of acute and chronic 900 MHz RF-EMR exposure on both passive avoidance behaviour and hippocampal levels of CaMKIIα and its phosphorylated form (pCaMKIIα). Rats were divided into the following groups: Sham rats, and rats exposed to 900 MHz RF-EMR for 2 h/day for 1 week (acute group) or 10 weeks (chronic group), respectively. Passive avoidance task was used as a behavioural method. The hippocampal levels of selected kinases were measured using Western Blotting technique. The results of passive avoidance task showed that both acute and chronic exposure to 900 MHz RF-EMR can impair passive avoidance behaviour with minor effects on chronic group of rats. The analysis of western blot data of selected protein kinases demonstrated that hippocampal levels of CaMKIIα and pCaMKIIα were significantly higher in chronic group of rats as compared to acute groups. Taken together, these findings demonstrated that different duration times (1 week vs 10 weeks) of 900 MHz RF-EMR exposure have different effects on both passive avoidance behaviour of rats and hippocampal levels of selected protein kinases.

Keywords: hippocampus, protein kinase, rat, RF-EMR

Procedia PDF Downloads 241

Authors: Shweta Verma

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Background: Epilepsy is a chronic non-communicable central nervous system (CNS) disorder which affects a large population of all ages. Different classes of drugs are used for the treatment of this neurological disorder, but due to augmented drug resistance and side effects, these drugs become incompetent. Therefore, we design the synthesis of ten new derivatives of Phenytoin. The moiety of Phenytoin was hybridized with different phenols by using three step approach. The synthesized molecules were then investigated for different physicochemical parameters, such as Log P values using diverse software programs and to predict the potential to cross the blood-brain barrier. Objective: The Phenytoin derivatives were designed, synthesized, and characterized to meet the structural necessities indispensable for antiepileptic activity. Method: Firstly, the chloroacetylation of the 5,5-diphenyl hydantoin was carried out, and then various substituted phenols were added to it. The synthesized compounds were characterized and evaluated for antianxiety activity by elevated plus maze method and antiepileptic activity by using subcutaneous pentylenetetrazole (scPTZ) and maximal electroshock (MES) models and neurotoxicity. Result: The number of derivatives of 5,5-diphenyl hydantoin was developed and optimized. The number of parameters was optimized which reveal that the compound containing chloro group such as C3 and C6 showed imperative potential when compared with the standard drug Diazepam. Other compounds containing nitro and methyl group were also found to possess activity. Conclusion: It was summarized that the new compounds of 5,5-diphenyl hydantoin derivatives were synthesized. The results of the data show that the compound containing chloro group is more potent for CNS activity. The new compounds have the probability of being optimized further to engender new scaffolds to treat various CNS disorders.

Keywords: phenytoin, parameters, CNS activity, blood-brain barrier, Log P, CNS active

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Authors: Sutapa Som Chaudhury, Chitrangada Das Mukhopadhyay

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Alzheimer’s disease is a well-known form of dementia since its discovery in 1906. Current Food and Drug Administration approved medications e.g. cholinesterase inhibitors, memantine offer modest symptomatic relief but do not play any role in disease modification or recovery. In last three decades many small molecules, chaperons, synthetic peptides, partial β-secretase enzyme blocker have been tested for the development of a drug against Alzheimer though did not pass the 3rd clinical phase trials. Here in this study, we designed a PEGylated, aminogenic, tripeptidic polymer with two different molecular weights based on the aggregation prone amino acid sequence 17-20 in amyloid beta (Aβ) 1-42. Being conjugated with poly-ethylene glycol (PEG) which self-assembles into hydrophilic nanoparticles, these PEGylated tripeptides constitute a very good drug delivery system crossing the blood brain barrier while the peptide remains protected from proteolytic degradation and non-specific protein interactions. Moreover, being completely aminogenic they would not raise any side effects. These peptide inhibitors were evaluated for their effectiveness against Aβ42 fibrillation at an early stage of oligomer to fibril formation as well as preformed fibril clearance via Thioflavin T (ThT) assay, dynamic light scattering analyses, atomic force microscopy and scanning electron microscopy. The inhibitors were proved to be safe at a higher concentration of 20µM by the reduction assay of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) dye. Moreover, SHSY5Y neuroblastoma cells have shown a greater survivability when treated with the inhibitors following Aβ42 fibril and oligomer treatment as compared with the control Aβ42 fibril and/or oligomer treated neuroblastoma cells. These make the peptidic inhibitors a promising compound in the aspect of the discovery of alternative medication for Alzheimer’s disease.

Keywords: Alzheimer’s disease, alternative medication, amyloid beta, PEGylated peptide

Procedia PDF Downloads 193