Search results for: phenolic compounds

Authors: Mehmet Doğan, Mahir Alkan, Yasemin Turhan, Zürriye Gündüz, Pinar Beyli, Serap Doğan

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Advances and new discoveries in the field of the material science on the basis of technological developments have played an important role. Today, material science is branched the lower branches such as metals, nonmetals, chemicals, polymers. The polymeric nano composites have found a wide application field as one of the most important among these groups. Many polymers used in the different fields of the industry have been desired to improve the thermal stability. One of the ways to improve this property of the polymers is to form the nano composite products of them using different fillers. There are many using area of boron compounds and is increasing day by day. In order to the further increasing of the variety of using area of boron compounds and industrial importance, it is necessary to synthesis of nano-products and to find yourself new application areas of these products. In this study, PMMA/boronoxide nano composites were synthesized using solution intercalation, polymerization and melting methods; and PAA/boronoxide nano composites using solution intercalation method. Furthermore, rheological properties of nano composites synthesed according to melting method were also studied. Nano composites were characterized by XRD, FTIR-ATR, DTA/TG, BET, SEM, and TEM instruments. The effects of filler material amount, solvent types and mediating reagent on the thermal stability of polymers were investigated. In addition, the rheological properties of PMMA/boronoxide nano composites synthesized by melting method were investigated using High Pressure Capillary Rheometer. XRD analysis showed that boronoxide was dispersed in polymer matrix; FTIR-ATR that there were interactions with boronoxide between PAA and PMMA; and TEM that boronoxide particles had spherical structure, and dispersed in nano sized dimension in polymer matrix; the thermal stability of polymers was increased with the adding of boronoxide in polymer matrix; the decomposition mechanism of PAA was changed. From rheological measurements, it was found that PMMA and PMMA/boronoxide nano composites exhibited non-Newtonian, pseudo-plastic, shear thinning behavior under all experimental conditions.

Keywords: boronoxide, polymer, nanocomposite, rheology, characterization

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Authors: Fatemeh Haghiralsadat, Mohadese Hashemi, Elham Akhoundi Kharanaghi, Mojgan Yazdani, Mahboobe Sharafodini, Omid Javani

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Niosomes are colloidal particles formed from the self-assembly of non-ionic surfactants in aqueous medium resulting in closed bilayer structures. As a consequence of this hydrophilic and hydrophobic structure, niosomes have the capacity to entrap compounds of different solubilities. Niosomes are promising vehicle for drug delivery which protect sensitive drugs and improve the therapeutic index of drugs by restricting their action to target cells. Essential oils are complex mixtures of volatile compounds such as terpenoids, phenol-derived aromatic components that have been used for many biological properties including bactericidal, fungicidal, insecticidal, antioxidant, anti-tyrosinase and other medicinal properties. Encapsulation of essential oils in niosomes can be an attractive method to overcome their limitation such as volatility, easily decomposition by heat, humidity, light, or oxygen. Cuminum cyminum L. (Cumin) is an aromatic plant included in the Apiaceae family and is used to flavor foods, added to fragrances, and for medical preparations which is indigenous to Egypt, the Mediterranean region, Iran and India. The major components of the Cumin oil were reported as cuminaldehyde, γ -terpinene, β-pinene, p-cymene, p-mentha-1, 3-dien-7-al, and p-mentha-1, 4-dien-7-al which provide the antimicrobial and antioxidant activity. The aim of this work was to formulate Cumin essential oil-loaded niosomes to improve water solubility of natural product and evaluate its physico-chemical features and stability. Cumin oil was obtained through steam distillation using a clevenger-type apparatus and GC/MS was applied to identify the main components of the essential oil. Niosomes were prepared by using thin film hydration method and nanoparticles were characterized for particle size, dispersity index, zeta potential, encapsulation efficiency, in vitro release, and morphology.

Keywords: Cuminum cyminum L., Cumin, niosome, essential oil, encapsulation

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Authors: P. Kiran Kumar, S. Vijaya Krishna, Kavita Verma1, V. Himabindu

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Concern about global warming and energy security has led to increased biomass utilization as an alternative feedstock to fossil fuels. Biomass is a promising feedstock since it is abundant and cheap and can be transformed into fuels and chemical products. Microalgae biofuels are likely to have a much lower impact on the environment. Microalgae cultivation using sewage with industrial flue gases is a promising concept for integrated biodiesel production, CO₂ sequestration, and nutrients recovery. Autotrophic, Mixotrophic, and Heterotrophic are the three modes of cultivation for microalgae biomass. Several mechanical and chemical processes are available for the extraction of lipids/oily components from microalgae biomass. In organic solvent extraction methods, a prior drying of biomass and recovery of the solvent is required, which are energy-intensive. Thus, the hydrothermal process overcomes the drawbacks of conventional solvent extraction methods. In the hydrothermal process, the biomass is converted into oily components by processing in a hot, pressurized water environment. In this process, in addition to the lipid fraction of microalgae, other value-added products such as proteins, carbohydrates, and nutrients can also be recovered. In the present study was (Scenedesmus quadricauda) was isolated and cultivated in autotrophic, heterotrophic, and mixotrophically using sewage wastewater and industrial flue gas in batch and continuous mode. The harvested algae biomass from S. quadricauda was used for the recovery of lipids and bio-oil. The lipids were extracted from the algal biomass using sonication as a cell disruption method followed by solvent (Hexane) extraction, and the lipid yield obtained was 8.3 wt% with Palmitic acid, Oleic acid, and Octadeonoic acid as fatty acids. The hydrothermal process was also carried out for extraction of bio-oil, and the yield obtained was 18wt%. The bio-oil compounds such as nitrogenous compounds, organic acids, and esters, phenolics, hydrocarbons, and alkanes were obtained by the hydrothermal process of algal biomass. Nutrients such as NO₃⁻ (68%) and PO₄⁻ (15%) were also recovered along with bio-oil in the hydrothermal process.

Keywords: flue gas, hydrothermal process, microalgae, sewage wastewater, sonication

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Authors: Habu Musa, Nusaibah Binti Syd Ali

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Oil palm industries particularly in Malaysia and Indonesia are being devastated by Ganoderma disease caused by Ganoderma spp. To date, this disease has been causing serious oil palm yield losses and collapse of oil palm trees, thus affecting its contribution to the producer’s economy. Research on sustainable and eco-friendly remedy to counter Ganoderma disease is on the upsurge to avoid the current control measures via synthetic fungicides. Trichoderma species have been the most studied and valued microbes as biological control agents in an effort to combat a wide range of plant diseases sustainably. Therefore, in this current study, the potential of Trichoderma spp. (Trichoderma asperellum, Trichoderma harzianum, and Trichoderma virens) as a consortium approach was evaluated as biological control agents against Ganoderma disease on oil palm. The consortium of Trichoderma spp. applied found to be the most effective treatment in suppressing Ganoderma disease with 83.03% and 89.16% from the foliar and bole symptoms respectively. Besides, it exhibited tremendous enhancement in the oil palm seedling vegetative growth parameters. Also, it had highly induced significant activity of peroxidase, polyphenol oxidase and total phenolic content was recorded in the consortium treatment compared to the control treatment. Disease development was slower in the seedlings treated with consortium of Trichoderma spp. compared to the positive control, which exhibited with the highest percentage of disease severity.

Keywords: biological control, ganoderma disease, trichoderma, disease severity

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Authors: S. Louhibi-Fasla, H. Rekab Djabri, H. Achour

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The aim of this work is to investigate the structural phase-transitions and electronic properties of copper halides. Our calculations were performed within the PLW extension to the first principle FPLMTO method, which enables an accurate treatment of all kinds of structures including the open ones. Results are given for lattice parameters, bulk modulus and its first derivatives in five different surface phases, and are compared with the available theoretical and experimental data. In the zinc-blende (B3) and PbO (B10) phases, the fundamental gap remains direct with both the top of VB and the bottom of CB located at Γ.

Keywords: FPLMTO, structural properties, Copper halides, phase transitions, ground state phase

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Authors: Nastaran Hazrati, Ali Akbar Miran Beigi, Majid Abdouss, Amir Vahid

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Hydrogen sulfide is the most toxic gas of crude oil. Adsorption is an energy-efficient process used to remove undesirable compounds such as H2S in gas or liquid streams by passing the stream through a media bed composed of an adsorbent. In this study, H2S of Iran crude oil was separated via cold stripping then zinc incorporated MCM-41 was synthesized via an in-situ method. ZnO functionalized mesoporous silica samples were characterized by XRD, N2 adsorption and TEM. The obtained results of adsorption of H2S showed superior ability of all the materials and with an increase in ZnO amount adsorption was increased.

Keywords: MCM-41, ZnO, H2S removal, adsorption

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Authors: Thouraya Majoul

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Obesity is now a real public health issue throughout the world, and it is well-established that obesity leads to cardiovascular diseases. The prevention and treatment of obesity using nutritional supplements has become a realistic and effective approach. This study was carried out to analyze the incidence of a high-fat diet on rat heart metabolism as well as on fatty acids composition, then to investigate the eventual protective effects of a grape seed extract (GSE). The experimental design consisted of three rat groups subjected to three different conditions; standard (SD), high-fat diet (HFD) and HFD+GSE (HG). We showed that GSE counteracted the effect of HFD on fatty acid composition, namely, docosapentaenoic acid, docosahexaenoic acid, arachidonic acid (ARA), palmitic acid (PA) and palmitoleic acid. Besides, GSE treatment restored HFD-altered metabolic pathways through the recovery of some cardiac enzyme activities such as lipase, glucose 6 phosphate dehydrogenase and pyruvate dehydrogenase. The cardiac lactate level and lactate dehydrogenase activity were also analyzed in relation to HFD and GSE administration. To our knowledge, this is the first study showing the anti-obesity and cardioprotective effects of GSE in relation to fatty acid composition and some cardiac enzymes, supporting its role as a therapeutic agent of obesity.

Keywords: Grape seed extract, phenolic, obesity, cardioprotective, lipotoxicity, energy metabolism

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Authors: A. T. Toci, M. V. B. Zanoni

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The advanced oxidation processes have been defined as destructive technologies treatment of wastewater. These involve the formation of powerful oxidizing agents (usually hydroxyl radical .OH) capable of reacting with organic compounds present in wastewater, transforming damaging substances in CO2 and H2O (mineralization) or other innocuous products. However, the photochemical degradation with singlet oxygen has been little explored as oxidative pathway for the treatment of effluents containing food colorants. The molecular oxygen is an effective suppressor of organic molecules in the triplet excited state. One of the possible results of the physical withdrawal is the formation of singlet oxygen. Studies with singlet oxygen (1O2) show an high reactivity of the excited state of the molecule with olefins, aromatic hydrocarbons and a number of other organic and inorganic compounds. Its reactivity is about 2500 times larger than the oxygen in the ground state. Thus, in this work, it was studied the degradation of some dyes used in food industry (tartrazine, sunset yellow, erythrosine and carmoisine) by singlet oxygen. The sensitizer used for generating the 1O2 was methylene blue, which has a quantum yield generation of 0.50. Samples were prepared in water at a concentration of 5 ppm and irradiated with a sunlight simulator (Newport brand, model no. 67005) by consecutive 8h. The absorption spectra of UV-Vis molecules were made each hour irradiation. The degradation kinetics for each dye was determined using the maximum length of each dye absorption. The analysis by UV-Vis revealed that the processes were very efficient for the colorants sunset yellow and carmoisine. Both presented degradation kinetics of order zero with degradation constants 0.416 and 0.104, respectively. In the case of sunset yellow degradation reached 53% after 7h irradiation, Demonstrating the process efficiency. The erithrosine presented during the period irradiated a oscillating degradation kinetics, which requires further study. In the other hand, tartrazine was stable in the presence of 1O2. The investigation of the dyes degradation products owned degradation by 1O2 are underway, the techniques used for this are MS and NMR. The results of this study will enable the application of the cleanest methods for the treatment of industrial effluents, as there are other non-toxic and polluting molecules to generate 1O2.

Keywords: food colourants, singlet oxygen, degradation, wastewater, oxidative

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Authors: Morgane Chatard, Clémentine Puech, Nathalie Perek, Frédéric Roche

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Several neurological disorders are linked to repeated hypoxia. The impact of such repeated hypoxic stress, on endothelial cells function of the blood-brain barrier (BBB) is little studied in the literature. Indeed, the study of hypoxic stress in cellular pathways is complex using hypoxia exposure because HIF 1α (factor induced by hypoxia) has a short half life. Our study presents an innovative induction method of repeated hypoxic stress, more reproducible, which allows us to study its impacts on an in vitro contact co-culture BBB model. Repeated hypoxic stress was induced by hydralazine (a mimetic agent of hypoxia pathway) during two hours and repeated during 24 hours. Then, BBB integrity was assessed by permeability measurements (transendothelial electrical resistance and membrane permeability), tight junction protein expressions (cell-ELISA and confocal microscopy) and by studying expression and activity of efflux transporters. First, this study showed that repeated hypoxic stress leads to a BBB’s dysfunction illustrated by a significant increase in permeability. This loss of membrane integrity was linked to a significant decrease of tight junctions’ protein expressions, facilitating a possible transfer of potential cytotoxic compounds in the brain. Secondly, we demonstrated that brain microvascular endothelial cells had set-up defence mechanism. These endothelial cells significantly increased the activity of their efflux transporters which was associated with a significant increase in their expression. In conclusion, repeated hypoxic stress lead to a loss of BBB integrity with a decrease of tight junction proteins. In contrast, endothelial cells increased the expression of their efflux transporters to fight against cytotoxic compounds brain crossing. Unfortunately, enhanced efflux activity could also lead to reducing pharmacological drugs delivering to the brain in such hypoxic conditions.

Keywords: BBB model, efflux transporters, repeated hypoxic stress, tigh junction proteins

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Authors: H. Alijani, M. Jabari, S. Matroodi, H. Zolqarnein, A. Sharafi, I. Zamani

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Actinomycetes, Gram-positive bacteria, are interesting as a main producer of secondary metabolites and are important industrially and pharmaceutically. The marine environment is a potential source for new actinomycetes, which can provide novel bioactive compounds and industrially important enzymes. The aims of this study were to isolate and identify novel actinomycetes from Persian Gulf sediments and screen these isolates for the production of secondary metabolites, especially antibiotics, Using phylogenetic (16S rRNA gene sequence), morphological and biochemical analyses. 15 different actinomycete strains from Persian Gulf sediments at a depth of 5-10 m were identified. DNA extraction was done using Cinnapure DNA Kit. PCR amplification of 16S rDNA gene was performed using F27 and R1492 primers. Phylogenetic tree analysis was performed using the MEGA 6 software. Most of the isolated strains belong to the genus namely Streptomyces (14), followed by Nocardiopsis (1). Antibacterial assay of the isolates supernatant was performed using a standard disc diffusion assay with replication (n=3). The results of disk diffusion assay showed that most active strain against Proteus volgaris and Bacillus cereus was AMJ1 (16.46±0.2mm and 13.78±0.2mm, respectively), against Salmonella sp. AMJ7 was the most effective strain (10.13±0.2mm), and AMJ1 and AHA5 showed more inhibitory activity against Escherichia coli (8.04±0.02 mm and 8.2±0.03 ). The AMJ6 strain showed best antibacterial activity against Klebsiella sp. (8.03±0.02mm). Antifungal activity of AMJ2 showed that it was most active strain against complex (16.05±0.02mm) and against Aspergillus flavus strain AMJ1 was most active strain (16.4±0.2mm) and highest antifungal activity against Trichophyton mentagrophytes, Microsporum gyp serum and Candida albicans, were shown by AHA1 (21.03±0.02mm), AHA3 and AHA7 (18±0.03mm), AMJ6 (21.03±0.2mm) respectively. Our results revealed that the marine actinomycetes of Persian Gulf sediments were potent source of novel antibiotics and bioactive compounds and indicated that the antimicrobial metabolites were extracellular. Most of the secondary metabolites and antibiotics are extracellular in nature and extracellular products of actinomycetes show potent antimicrobial activities.

Keywords: antibacterial activity, antifungal activity, marine actinomycetes, Persian Gulf

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Authors: Sonja Djilas, Gordana Ćetković, Jasna Čanadanović-Brunet, Vesna Tumbas Šaponjac, Slađana Stajčić, Jelena Vulić, Milica Vinčić

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In recent years, interest in food rich in bioactive compounds, such as polyphenols, increased the advantages of the functional food products. Bioactive components help to maintain health and prevention of diseases such as cancer, cardiovascular and many other degenerative diseases. Recent research has shown that the fruit pomace, a byproduct generated from the production of juice, can be a potential source of valuable bioactive compounds. The use of fruit industrial waste in the processing of functional foods represents an important new step for the food industry. Sour cherries have considerable nutritional, medicinal, dietetic and technological value. According to the production volume of cherries, Serbia ranks seventh in the world, with a share of 7% of the total production. The use of sour cherry pomace has so far been limited to animal feed, even though it can be potentially a good source of polyphenols. For this study, local variety of sour cherry cv. ‘Feketićka’ was chosen for its more intensive taste and deeper red color, indicating high anthocyanin content. The contents of total polyphenols, flavonoids and anthocyanins, as well as radical scavenging activity on DPPH radicals and reducing power of sour cherry juice and pomace were compared using spectrophotometrical assays. According to the results obtained, 66.91% of total polyphenols, 46.77% of flavonoids, 46.77% of total anthocyanins and 47.88% of anthocyanin monomers from sour cherry fruits have been transferred to juice. On the other hand, 29.85% of total polyphenols, 33.09% of flavonoids, 53.23% of total anthocyanins and 52.12% of anthocyanin monomers remained in pomace. Regarding radical scavenging activity, 65.51% of Trolox equivalents from sour cherries were exported to juice, while 34.49% was left in pomace. However, reducing power of sour cherry juice was much stronger than pomace (91.28% and 8.72% of Trolox equivalents from sour cherry fruits, respectively). Based on our results it can be concluded that sour cherry pomace is still a rich source of natural antioxidants, especially anthocyanins with coloring capacity, therefore it can be used for dietary supplements development and food fortification.

Keywords: antioxidants, polyphenols, pomace, sour cherry

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Authors: M. Ibrir, S. Berri, S. Lakel, D. Maouche And Y. Medkour

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We have performed first-principle calculations of the structural, electronic and magnetic properties of KFeF3, KCoF3, KMnF3, KVF3, using full-potential linearized augmented plane-wave (FP-LAPW) scheme within GGA. Features such as the lattice constant, bulk modulus and its pressure derivative are reported. Also, we have presented our results of the band structure and the density of states. The magnetic moments of KFeF3, KCoF3, KMnF3, KVF3 compounds are in most came from the exchange-splitting of X-3d orbital.

Keywords: Ab initio calculations, electronic structure, magnetic materials

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Authors: John Olayinka Atoyebi

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Developing countries like Nigeria are facing myriad problems, ranging from economic challenges, lack of no jobs, food insecurity, malnutrition, and poverty. However, tackling some of these menaces is not just a trivial issue neither do some of them require rocket science to fix, but rather the understanding of every individual citizen recognizing their respective roles that they have to play in making the country better, rather than putting all the blames on the Government. Tackling nutrition and food insecurity is a complex problem, but this work examines what an individual can do to improve nutrient consumption. Leafy indigenous vegetables can be termed as functional foods since they are very rich in nutrients, phytochemicals and other beneficial compounds to the body system. These functional foods are the class that provides necessary health benefits beyond basic nutrition. Usually functional foods often contain bioactive compounds, which help the body through the prevention and management of various diseases, as well as improving the overall health of human beings. The analysis carried out on some Nigerian leafy indigenous vegetables in home grown setting revealed, for example, the potential use of Iron (Fe) amount of 318.15ppm in Basella alba (red species) and that of Telfaria Occidentalis (Ugu) with 261.22ppm as being useful to stimulate heme, a necessary precursor and protein in the formation of blood in human being. Moreso, Virnonia amygdalina (ewuro) and water leaf possess anti-bacterial and anti-diabetic properties. They also provide digestive health benefits and support to the body system, including anti-inflammatory properties. Also, medicinal plant like Morinda citrifolia (Noni), which had been found to possess anti-cancer properties, has a Vitamin C amount of 528.85 mg/100g and a total carotenoids amount of 85.50 µg/g. However, despite all these results and potential utilization of these and other indigenous vegetables in Nigeria, there is a gross unawareness and/or non-cognizance of their utilization potentials, as some home garden lacks understanding of the immense nutrition benefits, thus hindering some of the populace to make proper use of these vegetables to enhance their health.

Keywords: developing countries, optimising, leafy vegetables, functional foods

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Authors: N. K. Fuloria, S. Fuloria, R. Gupta

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Esterification of p-bromo-m-cresol offered 2-(4-bromo-3-methyl phenoxy)acetate (1), which was hydrazinated to yield 2-(4-bromo-3-methyl phenoxy)aceto hydrazide (2). Compound (2) was reacted with different aromatic aldehydes to yield N-(substituted benzylidiene)-2-(4-bromo-3-methyl phenoxy)acetamide(3a-c). Cyclization of compound (3a-c) with thioglycolic acid yielded 2-(4-bromo-3-methylphenoxy)-N-(4-oxo-2-arylthiazolidin-3-yl) acetamide (4a-c). The newly synthesized compounds were characterized on the basis of spectral studies and evaluated for antibacterial and antifungal activities.

Keywords: imines, thiazolidinone, schiff base, antimicrobial

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Authors: V. Mani Rathnam, Giridhar Madras

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Fossil fuels are depleting rapidly as the demand for energy, and its allied chemicals are continuously increasing in the modern world. Therefore, sustainable renewable energy sources based on non-edible oils are being explored as a viable option as they do not compete with the food commodities. Oils such as castor oil are rich in fatty acids and thus can be used for the synthesis of biodiesel, bio-lubricants, and many other fine industrial chemicals. There are several processes available for the synthesis of different chemicals obtained from the castor oil. One such process is the transesterification of castor oil, which results in a mixture of fatty acid methyl esters. The main products in the above reaction are methyl ricinoleate and methyl 10-undecenoate. To separate these compounds, supercritical carbon dioxide (SCCO₂) was used as a green solvent. SCCO₂ was chosen as a solvent due to its easy availability, non-toxic, non-flammable, and low cost. In order to design any separation process, the preliminary requirement is the solubility or phase equilibrium data. Therefore, the solubility of a mixture of methyl ricinoleate with methyl 10-undecenoate in SCCO₂ was determined in the present study. The temperature and pressure range selected for the investigation were T = 313 K to 333 K and P = 10 MPa to 18 MPa. It was observed that the solubility (mol·mol⁻¹) of methyl 10-undecenoate varied from 2.44 x 10⁻³ to 8.42 x 10⁻³ whereas it varied from 0.203 x 10⁻³ to 6.28 x 10⁻³ for methyl ricinoleate within the chosen operating conditions. These solubilities followed a retrograde behavior (characterized by the decrease in the solubility values with the increase in temperature) throughout the range of investigated operating conditions. An association theory model, coupled with regular solution theory for activity coefficients, was developed in the present study. The deviation from the experimental data using this model can be quantified using the average absolute relative deviation (AARD). The AARD% for the present compounds is 4.69 and 8.08 for methyl 10-undecenoate and methyl ricinoleate, respectively in a mixture of methyl ricinoleate and methyl 10-undecenoate. The maximum solubility enhancement of 32% was observed for the methyl ricinoleate in a mixture of methyl ricinoleate and methyl 10-undecenoate. The highest selectivity of SCCO₂ was observed to be 12 for methyl 10-undecenoate in a mixture of methyl ricinoleate and methyl 10-undecenoate.

Keywords: association theory, liquid mixtures, solubilities, supercritical carbon dioxide

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Authors: Palaniyandi Karuppaiya, Hsin Sheng Tsay, Fang Chen

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Medicinal herbs do represent a huge and noteworthy reservoir for novel anticancer drugs discovery. Dysosma pleiantha (Hance) Woodson (Berberidaceae), one of the oldest traditional Chinese medicinal herb, highly prized by the mountain tribes of Taiwan and China for its medicinal properties contained pharmaceutically important antitumor compounds podophyllotoxin, quercetin and kaempferol. Among lignans, podophyllotoxin is an active antitumor compound and has now been modified to produce clinically useful drugs etoposide and teniposide. In recent years, natural populations of D. peliantha have declined considerably due to anthropogenic activities such as habitat destruction and commercial exploitation for medicinal applications. As to its overall conservation status, D. pleiantha has been ranked as threatened on the China Species Red List. In the present study, an efficient in vitro callus culture system of D. pleiantha was established on Gamborg’s medium with various combinations and concentrations of different auxins and cytokinins under dark condition. Best callus induction was recorded in 2 mg/L 2, 4 - Dichlorophenoxyacetic acid (2,4-D) along with 0.2 mg/L kinetin and the maximum callus proliferation was achieved at 1 mg/L 2,4-D. Among the explants tested, maximum callus induction (86 %) was achieved from tender leaves. Hence, in subsequent experiments, leaf callus was further investigated for suitable callus biomass and production level of anticancer compounds under the influence of different additives. A maximum fresh callus biomass (8.765 g) was recorded in callus proliferation medium contained 500 mg/L casein hydrolysate. High performance liquid chromatography results revealed that the addition of different concentrations of peptone (1, 2 and 4 g/L) in callus proliferation medium enhanced podophyllotoxin (16 fold), quercetin (12 fold) and kaempferol (5 fold) accumulation than control. Thus, the established in vitro callus culture under the influence of different additives may offer an alternative source of enhanced production of podophyllotoxin, kaempferol and quecertin without harming natural plant population.

Keywords: dysosma pleiantha, kaempferol, podophyllotoxin, quercetin

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Authors: T. Ould Bellahcen, A. Amiri, I. Touam, F. Hmimid, A. El Amrani, M. Cherki

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The antioxidant activity of three extracts (water, lipidic and ethanolic) prepared from the microalgae Spirulina platensis isolated from Moroccan lake, using 2, 2 diphenyl-1-picrylhydrazyl (DPPH) and 2,2’-azino-bis ethylbenzthiazoline-6-sulfonic acid (ABTS) radical assay, was studied and compared. The obtained results revealed that the IC₅₀ found using DPPH were lower than that of ABTS for all extracts from these planktonic blue-green algae. The high levels of phenolic and flavonoid content were found in the ethanolic extract 0,33 ± 0,01 mg GAE/g dw and 0,21 ± 0,01 mg quercetin/g dw respectively. In addition, using DPPH, the highest activity with IC₅₀ = 0,449 ± 0,083 mg/ml, was found for the ethanolic extract, followed by that of lipidic extract (IC₅₀ = 0,491 ± 0,059 mg/ml). The lowest activity was for the aqueous extract (IC₅₀ = 4,148 ± 0,132 mg/ml). For ABTS, the highest activity was observed for the lipidic extract with IC₅₀ = 0,740 ± 0,012 mg/ml, while, the aqueous extract recorded the lowest activity (IC₅₀ = 6,914 ± 0, 0067 mg/ml). A moderate activity was showed for the ethanolic extract (IC₅₀ = 5,852 ± 0, 0171 mg/ml). It can be concluded from this first study that Spirulina platensis extracts show an interesting antioxidant and antiradicals properties suggesting that this alga could be used as a potential source of antioxidants. A qualitative and quantitative analysis of polyphenol and flavonoids in the extracts using HPLC is in progress so as to study the correlation between the antioxidant activity and chemical composition.

Keywords: Spirulina platensis, antioxidant, DPPH, ABTS

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Authors: Hummera Rafique, Aamer Saeed

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2-Aminobenzothiazoles are highly biologically active compounds, as many important applications are associated with this nucleus. They serve as precursors for the synthesis of thioureas. Benzothiazolyl thioureas are exceptionally versatile building blocks towards the synthesis of a wide variety of heterocyclic systems, which also possess extensive range of bioactivities. These thioureas were converted into five-membered heterocycles with imino moiety like N-[3-(2-Benzothiazolyl)-4-methylthiazol-2(3H)-ylidene] benzamides by base-catalyzed cyclization of corresponding thioureas with 2-bromoacetone and triethylamine in good yields.

Keywords: N-[3-(2-Benzothiazolyl)-4-methylthiazol-2(3H)-ylidene]benzamides, 1-(substitutedbenzo[d] thiazol-2-yl)-3-aroylthioureas, 2-aminobenzothiazoles, antibacterial activities

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Authors: Sheraz Gul

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The requirements for progressing a compound to clinical trials is well established and relies on the results from in-vitro and in-vivo animal tests to indicate that it is likely to be safe and efficacious when testing in humans. The typical data package required will include demonstrating compound safety, toxicity, bioavailability, pharmacodynamics (potential effects of the compound on body systems) and pharmacokinetics (how the compound is potentially absorbed, distributed, metabolised and eliminated after dosing in humans). If the desired criteria are met and the compound meets the clinical Candidate criteria and is deemed worthy of further development, a submission to regulatory bodies such as the US Food & Drug Administration for an exploratory Investigational New Drug Study can be made. The purpose of this study is to collect data to establish that the compound will not expose humans to unreasonable risks when used in limited, early-stage clinical studies in patients or normal volunteer subjects (Phase I). These studies are also designed to determine the metabolism and pharmacologic actions of the drug in humans, the side effects associated with increasing doses, and, if possible, to gain early evidence on their effectiveness. In order to reach the above goals, we have developed a pre-clinical high throughput Absorption, Distribution, Metabolism and Excretion–Toxicity (ADME–Toxicity) panel of assays to identify compounds that are likely to meet the Lead and Candidate compound acceptance criteria. This panel includes solubility studies in a range of biological fluids, cell viability studies in cancer and primary cell-lines, mitochondrial toxicity, off-target effects (across the kinase, protease, histone deacetylase, phosphodiesterase and GPCR protein families), CYP450 inhibition (5 different CYP450 enzymes), CYP450 induction, cardio-toxicity (hERG) and gene-toxicity. This panel of assays has been applied to multiple compound series developed in a number of projects delivering Lead and clinical Candidates and examples from these will be presented.

Keywords: absorption, distribution, metabolism and excretion–toxicity , drug discovery, food and drug administration , pharmacodynamics

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Authors: Muhammad Atif Randhawa, Mahreen Akhtar, Sidrah

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In this paper, Jamun (Syzygium cumini; Myrtaceae) drink enriched with jamun pulp and seed was assessed for different physicochemical parameters (titratable acidity, pH, TSS, ascorbic acid, and total sugars and reducing sugars) and phytochemical aspects at every 15 days interval till 60 days storage period. Jamun pulp both with seed and without seed were used at levels of 7, 10 and 13 percent to prepare jamun drink in six combinations; T1 (7% pulp without seed), T2 (10% pulp without seed), T3 (13% pulp without seed), T4 (7% pulp with seed), T5 (10% pulp with seed), T6 (13% pulp with seed). Storage period resulted decrease in pH (4.18 to 4.08) and ascorbic acid (21.92%) significantly along with phenolic contents (6.13 to 4.85g of GAE/kg) and antioxidant activity (70.68 to 48.62 percent) within treatments. All treatments showed significant increases in total sugars (11.59 to 11.80%), reducing sugars (2.30 to 2.50%), TSS (12.2 to 13.32 °B) and acidity (0.23% to 0.31%) during storage. Treatments T3, T5 and T6 showed best results in terms of all physicochemical parameters during storage. Statistically significant differences were obtained among sensory parameters as a function of pulp type and concentration, while treatment T5 (10% pulp with seed) obtained highest score (7.16) in terms of all sensory parameters. It can be concluded that nutrient rich jamun drink can be prepared as an attempt to add value to the underutilized jamun fruit of Pakistan.

Keywords: antioxidant activity, Jamun beverage, physicochemical, storage

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Authors: Ahilya Singh, Brad Carte, Ramesh Subramani, William Aalbersberg

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A total of 37 actinomycete strains were purified from 25 Solomon Islands marine sediments using four different types of isolation media. Among them, 54% of the strains had obligate requirement of seawater for growth. The ethyl acetate extract of 100 ml fermentation product of each strain was screened for antimicrobial activity against multidrug resistant human pathogens and cytotoxic activity against brine shrimps. A total of 67% of the ethyl acetate extracts showed antimicrobial and/or cytotoxic activities. A strain F-1915 was selected for isolation and evaluation of bioactive compound(s) based on its bioactive properties and chemical profile analysis using the LC-MS. The strain F-1915 was identified to have 96% sequence similarity to Streptomyces violaceusniger on the basis of 16S rDNA sequences using BLAST analysis. The 16S rDNA revealed that the strain F-1915 is a new member of MAR4 clade of actinomycetes. The MAR4 clade is an interesting clade of actinomycetes known for the production of pharmaceutically important hybrid isoprenoid compounds. The ethyl acetate extract of the fermentation product of this strain was purified by silica gel column chromatography and afforded the isolation of one bioactive pure compound. Based on the 1D and 2D NMR spectral data of compound 1 it was identified as a new mono-brominated phenazinone, Marinophenazimycin A, a structure which has already been studied by external collaborators at Scripps Institution of Oceanography but is yet to be published. Compound 1 displayed significant antimicrobial activity against drug resistant human pathogens. The minimum inhibitory concentration (MIC) of compound 1 was against Methicillin Resistant Staphylococcus aureus (MRSA) was about 1.9 μg/ml and MIC recorded against Amphotericin Resistant Candida albicans (ARCA) was about 0.24 μg/ml. The bioactivity of compound 1 against ARCA was found to be better than the standard antifungal agent amphotericin B. Compound 1 however did not show any cytotoxic activity against brine shrimps.

Keywords: actinomycetes, antimicrobial activity, brominated phenazine, MAR4 clade, marine natural products, multidrug resistent, 1D and 2D NMR

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Authors: K. Akutsu, S. Mori, T. Hanashima

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Fluorescent probes are useful for the selective detection of trace amount of ions and biomolecular imaging in living cells. Various kinds of metal ion-selective fluorescent compounds have been developed, and some compounds have been applied as effective metal ion-selective fluorescent probes. However, because competition between the ligand and water molecules for the metal ion constitutes a major contribution to the stability of a complex in aqueous solution, it is difficult to develop a highly sensitive, selective, and stable fluorescent probe in aqueous solution. The micelles, these are formed in the surfactant aqueous solution, provides a unique hydrophobic nano-environment for stabilizing metal-organic complexes in aqueous solution. Therefore, we focused on the unique properties of micelles to develop a new fluorescence analysis system. We have been developed a fluorescence analysis system for Sr(II) by using a Sr(II) fluorescent sensor, N-(2-hydroxy-3-(1H-benzimidazol-2-yl)-phenyl)-1-aza-18-crown-6-ether (BIC), and studied its complexation behavior with Sr(II) in micellar solution. We revealed that the stability constant of Sr(II)-BIC complex was 10 times higher than that in aqueous solution. In addition, its detection limit value was also improved up to 300 times by this system. However, the mechanisms of these phenomena have remained obscure. In this study, we investigated the structure of Sr(II)-BIC complex in aqueous micellar solution by combining use the extended X-ray absorption fine structure (EXAFS) and neutron reflectivity (NR) method to understand the unique properties of the fluorescence analysis system from the view point of structural chemistry. EXAFS and NR experiments were performed on BL-27B at KEK-PF and on BL17 SHARAKU at J-PARC MLF, respectively. The obtained EXAFS spectra and their fitting results indicated that Sr(II) and BIC formed a Sr(18-crown-6-ether)-like complex in aqueous micellar solution. The EXAFS results also indicated that the hydrophilic head group of surfactant molecule was directly coordinated with Sr(II). In addition, the NR results also indicated that Sr(II)-BIC complex would interact with the surface of micelle molecules. Therefore, we concluded that Sr(II), BIC, and surfactant molecule formed a ternary complexes in aqueous micellar solution, and at least, it is clear that the improvement of the stability constant in micellar solution is attributed to the result of the formation of Sr(BIC)(surfactant) complex.

Keywords: micell, fluorescent probe, neutron reflectivity, EXAFS

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Authors: Vesta Kohlmeier, George C. Dragan, Juergen Orasche, Juergen Schnelle-Kreis, Dietmar Breuer, Ralf Zimmermann

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Aerosols from hazardous semi-volatile organic compounds (SVOC) may occur in workplace air and can simultaneously be found as particle and gas phase. For health risk assessment, it is necessary to collect particles and gases separately. This can be achieved by using a denuder for the gas phase collection, combined with a filter and an adsorber for particle collection. The study focused on the suitability of carbonaceous monolithic multi-channel denuders, so-called Novacarb™-Denuders (MastCarbon International Ltd., Guilford, UK), to achieve gas-particle separation. Particle transmission efficiency experiments were performed with polystyrene latex (PSL) particles (size range 0.51-3 µm), while the time dependent gas phase collection efficiency was analysed for polar and nonpolar SVOC (mass concentrations 7-10 mg/m3) over 2 h at 5 or 10 l/min. The experimental gas phase collection efficiency was also compared with theoretical predictions. For n-hexadecane (C16), the gas phase collection efficiency was max. 91 % for one denuder and max. 98 % for two denuders, while for diethylene glycol (DEG), a maximal gas phase collection efficiency of 93 % for one denuder and 97 % for two denuders was observed. At 5 l/min higher gas phase collection efficiencies were achieved than at 10 l/min. The deviations between the theoretical and experimental gas phase collection efficiencies were up to 5 % for C16 and 23 % for DEG. Since the theoretical efficiency depends on the geometric shape and length of the denuder, flow rate and diffusion coefficients of the tested substances, the obtained values define an upper limit which could be reached. Regarding the particle transmission through the denuders, the use of one denuder showed transmission efficiencies around 98 % for 1-3 µm particle diameters. The use of three denuders resulted in transmission efficiencies from 93-97 % for the same particle sizes. In summary, NovaCarb™-Denuders are well applicable for sampling aerosols of polar/nonpolar substances with particle diameters ≤3 µm and flow rates of 5 l/min or lower. These properties and their compact size make them suitable for use in personal aerosol samplers. This work is supported by the German Social Accident Insurance (DGUV), research contract FP371.

Keywords: gas phase collection efficiency, particle transmission, personal aerosol sampler, SVOC

Procedia PDF Downloads 176

Authors: Archana Gupta, Rajesh Kumar

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The chemistry of chalcones has generated intensive scientific studies throughout the world. Especially, interest has been focused on the synthesis and biodynamic activities of chalcones. The blue light transmittance, excellent crystallizability and the two planar rings connected through a conjugated double bond show that chalcone derivatives are superior nonlinear organic compounds. 3-(2-Chloro-6-fluoro¬phen¬yl)-1-(2-thien¬yl) prop-2-en-1-one, 3-(2, 4- Dichlorophenyl) – 1 - (4-methylphenyl) – prop -2-en-1-one, (2E)-3-[4-(methylsulfanyl) phenyl]-1-(4-nitrophenyl) prop-2-en-1-one are some chalcone derivatives exhibiting non linear optical (NLO) properties. NLO materials have been extensively investigated in recent years as they are the key elements for photonic technologies of optical communication, optical interconnect oscillator, amplifier, frequency converter etc. Due to their high molecular hyperpolarizabilities, organic materials display a number of significant NLO properties. Experimental measurements and theoretical calculations on molecular hyperpolarizability β have become one of the key factors in the design of second order NLO materials. Theoretical determination of hyperpolarizability is quite useful both in understanding the relationship between the molecular structure and NLO properties. It also provides a guideline to experimentalists for the design and synthesis of organic NLO materials. Quantum-chemical calculations have made an important contribution to the understanding of the electronic polarization underlying the molecular NLO processes and the establishment of structure–property relationships. In the present investigation, the detailed vibrational analysis of some chalcone derivatives is taken up to understand the correlation of the charge transfer interaction and the NLO activity of the molecules based on density functional theory calculations. The vibrational modes contributing toward the NLO activity have been identified and analyzed. Rather large hyperpolarizability derived by theoretical calculations suggests the possible future use of these compounds for non-linear optical applications. The study suggests the importance of π - conjugated systems for non-linear optical properties and the possibility of charge transfer interactions. We hope that the results of the present study of chalcone derivatives are of assistance in development of new efficient materials for technological applications.

Keywords: hyperpolarizability, molecular structure, NLO material, quantum chemical calculations

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Authors: Mekhaldi Abdelkader, Bouzned Ahcen, Djibaoui Rachid, Hamoum Hakim

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This study presents an attempt to evaluate the antioxidant and antimicrobial activity of methanolic extract and essential oils prepared from the leaves of sage (Salvia officinalis L.). The content of polyphenols in the methanolic extract of the leaves from Salvia officinalis extract was determined by spectrophoto- metrically, calculated as gallic acid and catechin equivalent. Antioxidant activity was evaluated by free radical scavenging activity using 2,2-diphenylpicryl-1-picrylhydrazyl (DPPH) assay. The plant essential oil and methanol extract were also subjected to screenings for the evaluation of their antioxidant activities using 2, 2-diphenyl-1-picrylhydrazyl (DPPH) test. While the plant essential oil showed only weak antioxidant activities, its methanol extract was considerably active in DPPH (IC50= 37.29µg/ml) test. Appreciable total phenolic content (31.25mg/g) was also detected for the plant methanol extract as gallic acid equivalent in the Folin–Ciocalteu test. The plant was also screened for its antimicrobial activity and good to moderate inhibitions were recorded for its essential oil and methanol extract against most of the tested microorganisms. The present investigation revealed that this plant has rich source of antioxidant properties. It is for this reason that sage has found increasing application in food formulations.

Keywords: antibacterial activity, antioxidant activity, flavonoid, polyphenol, salvia officinalis

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Authors: Cristina Núñez, Rufina Bastida, Elena Labisbal, Alejandro Macías, María T. Pereira, José M. Vila

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A highly selective quinoline-based fluorescent sensor L was designed in order to functionalize gold nanoparticles (GNPs@L). The cytotoxicity of compound L and GNPs@L on the MCF-7 breast cancer cells was explored and it was observed that L and GNPs@L compounds induced apoptosis in MCF-7 cancer cells. The cellular uptake of the hybrid system GNPs@L was studied using confocal laser scanning microscopy (CLSM).

Keywords: cytotoxicity, fluorescent probes, nanoparticles, quinoline

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Authors: Mohammed Nasir Kajama, Ngozi Claribelle Nwogu, Edward Gobina

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Pt/γ-Al2O3 membrane catalysts were prepared via an evaporative-crystallization deposition method. The obtained Pt/γ-Al2O3 catalyst activity was tested after characterization (SEM-EDAX observation, BET measurement, permeability assessment) in the catalytic oxidation of selected volatile organic compound (VOC) i.e. propane, fed in mixture of oxygen. The VOC conversion (nearly 90%) obtained by varying the operating temperature showed that flow-through membrane reactor might do better in the abatement of VOCs.

Keywords: VOC combustion, flow-through membrane reactor, platinum supported alumina catalysts

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Authors: M. Abdoul-Hakim, A. Zeroual, H. Garmes

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2-Chlorobenzimidazoles are amphoteric compounds and versatile intermediates for the construction of polycyclic heterocycles. In this theoretical study performed by DFT at the B3LYP/6-311+G(d,p) level, we showed that the most likely route to obtain benzimidazo[1,2-d]oxadiazole from the reaction of 2-Chlorobenzimidazole with benzonitrile N-oxide involves the presence of anionic species, a concerted mechanism is not possible. The inclusion of the effect of the polar protic solvent (MeOH) favors the course of the reaction. The key interactions causing bond formation and breakage were identified by ELF topological analysis.

Keywords: benzimidazo[1, 2-d]oxadiazole, benzonitrile N-oxide, DFT, ELF, polycyclic heterocycles

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Authors: Nassima Behidj-Benyounes, Thoraya Dahmene

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Essential oils have a significant antimicrobial activity. These oils can successfully replace the antibiotics. So, the microorganisms show their inefficiencies resistant for the antibiotics. For this reason, we study the physic-chemical analysis and antimicrobial activity of the essential oil of Daucus carota. The extraction is done by steam distillation of water which brought us a very significant return of 4.65%. The analysis of the essential oil is performed by GC/MS and has allowed us to identify 32 compounds in the oil of D. carota flowering tops of Bouira. Three of which are in the majority are the α-pinene (22.3%), the carotol (21.7%) and the limonene (15.8%).

Keywords: daucus carota, essential oil, α-pinene, carotol, limonene

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Authors: K. Eryilmaz, G. Mercanoglu

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Aim: Purification of the final product, which is the last step in the synthesis of lanthanide-labeled peptide compounds, can be accomplished by different methods. Among these methods, the two most commonly used methods are C18 solid phase extraction (SPE) and weak cation exchanger cartridge elution. SPE C18 solid phase extraction method yields high purity final product, while elution from the weak cation exchanger cartridge is pH dependent and ineffective in removing colloidal impurities. The aim of this work is to develop an additional purification method for the lanthanide-labeled peptide compound in cases where the desired radionuclidic and radiochemical purity of the final product can not be achieved because of pH problem or colloidal impurity. Material and Methods: For colloidal impurity formation, 3 mL of water for injection (WFI) was added to 30 mCi of 177LuCl3 solution and allowed to stand for 1 day. 177Lu-DOTATATE was synthesized using EZAG ML-EAZY module (10 mCi/mL). After synthesis, the final product was mixed with the colloidal impurity solution (total volume:13 mL, total activity: 40 mCi). The resulting mixture was trapped in SPE-C18 cartridge. The cartridge was washed with 10 ml saline to remove impurities to the waste vial. The product trapped in the cartridge was eluted with 2 ml of 50% ethanol and collected to the final product vial via passing through a 0.22μm filter. The final product was diluted with 10 mL of saline. Radiochemical purity before and after purification was analysed by HPLC method. (column: ACE C18-100A. 3µm. 150 x 3.0mm, mobile phase: Water-Acetonitrile-Trifluoro acetic acid (75:25:1), flow rate: 0.6 mL/min). Results: UV and radioactivity detector results in HPLC analysis showed that colloidal impurities were completely removed from the 177Lu-DOTATATE/ colloidal impurity mixture by purification method. Conclusion: The improved purification method can be used as an additional method to remove impurities that may result from the lanthanide-peptide synthesis in which the weak cation exchange purification technique is used as the last step. The purification of the final product and the GMP compliance (the final aseptic filtration and the sterile disposable system components) are two major advantages.

Keywords: lanthanide, peptide, labeling, purification, radionuclide, radiopharmaceutical, synthesis

Procedia PDF Downloads 160