Search results for: decarboxylative radical cyclization
Commenced in January 2007
Frequency: Monthly
Edition: International
Paper Count: 662

Search results for: decarboxylative radical cyclization

572 Compositional Analysis and Antioxidant Activities of the Chocolate Fermented by Lactobacillus plantarum CK10

Authors: Hye Rim Kang, So Yae Koh, Ji-Yeon Ryu, Chang Kyu Lee, Ji Hee Lim, Hyeon A. Kim, Geun Hyung Im, Somi Kim Cho

Abstract:

In this study, antioxidant properties and compositional analysis of fermented chocolate were examined. Chocolate was fermented with Lactobacillus plantarum CK10. As fermentation time went by, pH was decreased (5.26±0.02 to 3.98±0.06) while titratable acidity was increased (5.36±0.19 to 13.31±0.34). The total polyphenol contents were maintained through the fermentation. The contents of total polyphenol were slightly increased at 8 hr (6.34±0.12 mg GAE (Gallic acid equivalent)/g), and it reached to comparable levels of the control at 24 hr (control, 5.47±0.36 mg GAE/g); 24 hr, 5.19±0.23 mg GAE/g). Similarly, the total flavonoid contents were not significantly changed during fermentation. The pronounced radical scavenging activities of chocolate, against DPPH-, ABTS-, and Alkyl radical, were observed. The levels of antioxidant activities were not dramatically altered in the course of fermentation. By gas chromatography-mass spectrometry analysis, the increase in lactic acid was measured and four major compounds, HMF, xanthosine, caffeine, and theobromine, were identified. The relative peak area of caffeine and theobromine was considerably changed during fermentation. However, no significant difference in the levels of caffeine and theobromine were observed by high-performance liquid chromatography analysis.

Keywords: antioxidant, chocolate, compositional analysis, fermentation, Lactobaillus plantarum

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571 The Effect of Primary Treatment on Histopathological Patterns and Choice of Neck Dissection in Regional Failure of Nasopharyngeal Carcinoma Patients

Authors: Ralene Sim, Stefan Mueller, N. Gopalakrishna Iyer, Ngian Chye Tan, Khee Chee Soo, R. Shetty Mahalakshmi, Hiang Khoon Tan

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Background: Regional failure in nasopharyngeal carcinoma (NPC) is managed by salvage treatment in the form of neck dissection. Radical neck dissection (RND) is preferred over modified radical neck dissection (MRND) since it is traditionally believed to offer better long-term disease control. However, with the advent of more advanced imaging modalities like high-resolution Magnetic Resonance Imaging, Computed Tomography, and Positron Emission Tomography-CT scans, earlier detection is achieved. Additionally, concurrent chemotherapy also contributes to reduced tumour burden. Hence, there may be a lesser need for an RND and a greater role for MRND. With this retrospective study, the primary aim is to ascertain whether MRND, as opposed to RND, has similar outcomes and hence, whether there would be more grounds to offer a less aggressive procedure to achieve lower patient morbidity. Methods: This is a retrospective study of 66 NPC patients treated at Singapore General Hospital between 1994 to 2016 for histologically proven regional recurrence, of which 41 patients underwent RND and 25 who underwent MRND, based on surgeon preference. The type of ND performed, primary treatment mode, adjuvant treatment, and pattern of recurrence were reviewed. Overall survival (OS) was calculated using Kaplan-Meier estimate and compared. Results: Overall, the disease parameters such as nodal involvement and extranodal extension were comparable between the two groups. Comparing MRND and RND, the median (IQR) OS is 1.76 (0.58 to 3.49) and 2.41 (0.78 to 4.11) respectively. However, the p-value found is 0.5301 and hence not statistically significant. Conclusion: RND is more aggressive and has been associated with greater morbidity. Hence, with similar outcomes, MRND could be an alternative salvage procedure for regional failure in selected NPC patients, allowing similar salvage rates with lesser mortality and morbidity.

Keywords: nasopharyngeal carcinoma, neck dissection, modified neck dissection, radical neck dissection

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570 In Vitro Antioxidant Properties of Balanites Aeqyptiaca Del Enzymatic Protein Hydrolysates

Authors: Friday A. Ogori, Ojotu M. Eke, Oneh J. Abu, Abraham T. Girgih

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B.aeqygtiaca del (Balanites aegyptiaca del) seed protein concentrate (APC) was hydrolyzed using different enzymes such as pepsin+pancreatin (PP), Alcalase (Alca), and Flavourzyme (Flav). The Alca has higher yield (100%) when compared to PP (83.23%) and Flav (62.90%). The hydrophobic amino acid and Sulphur containing amino acid (40.19%, 7.04%) in PP hydrolysate were higher compared to Alcalase (38.92%, 6.69%), Flavourenzyme (37.43%,6.35%), and APC (39.97%, 6.95%) samples. The PP has stronger DPPH, Hydroxyl radical quenching, Ferric reducing activity, and linoleic acid peroxidation activity, followed by the protein concentrate (APC) and Alcalase (Alca), while Flavourenzyme (Flav) derived hydrolysate was least in scavenging and inhibiting radical peroxidation properties. Flavourenzyme derived hydrolysate had stronger Ferric reducing antioxidant potential and metal chelating property. The result showed that the Alcalase hydrolysate has promising peptide yield, and PP hydrolysate had excellent amino acid residues and good in-vitro antioxidant potentials and could be a preferred ingredients in the nutraceutical and functional food emerging industries.

Keywords: balanites aegyptiaca del, protein concentrate, protein hydrolysates, enzymatic hydrolysis, antioxidants

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569 The Effects of in vitro Digestion on Cheese Bioactivity; Comparing Adult and Elderly Simulated in vitro Gastrointestinal Digestion Models

Authors: A. M. Plante, F. O’Halloran, A. L. McCarthy

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By 2050 it is projected that 2 billion of the global population will be more than 60 years old. Older adults have unique dietary requirements and aging is associated with physiological changes that affect appetite, sensory perception, metabolism, and digestion. Therefore, it is essential that foods recommended and designed for older adults promote healthy aging. To assess cheese as a functional food for the elderly, a range of commercial cheese products were selected and compared for their antioxidant properties. Cheese from various milk sources (bovine, goats, sheep) with different textures and fat content, including cheddar, feta, goats, brie, roquefort, halloumi, wensleydale and gouda, were initially digested with two different simulated in vitro gastrointestinal digestion (SGID) models. One SGID model represented a validated in vitro adult digestion system and the second model, an elderly SGID, was designed to consider the physiological changes associated with aging. The antioxidant potential of all cheese digestates was investigated using in vitro chemical-based antioxidant assays, (2,2-Diphenyl-1-picrylhydrazyl (DPPH) radical scavenging, ferric reducing antioxidant power (FRAP) and total phenolic content (TPC)). All adult model digestates had high antioxidant activity across both DPPH ( > 70%) and FRAP ( > 700 µM Fe²⁺/kg.fw) assays. Following in vitro digestion using the elderly SGID model, full-fat red cheddar, low-fat white cheddar, roquefort, halloumi, wensleydale, and gouda digestates had significantly lower (p ≤ 0.05) DPPH radical scavenging properties compared to the adult model digestates. Full-fat white cheddar had higher DPPH radical scavenging activity following elderly SGID digestion compared to the adult model digestate, but the difference was not significant. All other cheese digestates from the elderly model were comparable to the digestates from the adult model in terms of radical scavenging activity. The FRAP of all elderly digestates were significantly lower (p ≤ 0.05) compared to the adult digestates. Goats cheese was significantly higher (p ≤ 0.05) in FRAP (718 µM Fe²/kg.fw) compared to all other digestates in the elderly model. TPC levels in the soft cheeses (feta, goats) and low-fat cheeses (red cheddar, white cheddar) were significantly lower (p ≤ 0.05) in the elderly digestates compared to the adult digestates. There was no significant difference in TPC levels, between the elderly and adult model for full-fat cheddar (red, white), roquefort, wensleydale, gouda, and brie digestates. Halloumi cheese was the only cheese that was significantly higher in TPC levels following elderly digestion compared to adult digestates. Low fat red cheddar had significantly higher (p ≤ 0.05) TPC levels compared to all other digestates for both adult and elderly digestive systems. Findings from this study demonstrate that aging has an impact on the bioactivity of cheese, as antioxidant activity and TPC levels were lower, following in vitro elderly digestion compared to the adult model. For older adults, soft cheese, particularly goats cheese, was associated with high radical scavenging and reducing power, while roquefort cheese had low antioxidant activity. Also, elderly digestates of halloumi and low-fat red cheddar were associated with high TPC levels. Cheese has potential as a functional food for the elderly, however, bioactivity can vary depending on the cheese matrix. Funding for this research was provided by the RISAM Scholarship Scheme, Cork Institute of Technology, Ireland.

Keywords: antioxidants, cheese, in-vitro digestion, older adults

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568 Degradation of Emerging Pharmaceuticals by Gamma Irradiation Process

Authors: W. Jahouach-Rabai, J. Aribi, Z. Azzouz-Berriche, R. Lahsni, F. Hosni

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Gamma irradiation applied in removing pharmaceutical contaminants from wastewater is an effective advanced oxidation process (AOP), considered as an alternative to conventional water treatment technologies. In this purpose, the degradation efficiency of several detected contaminants under gamma irradiation was evaluated. In fact, radiolysis of organic pollutants in aqueous solutions produces powerful reactive species, essentially hydroxyl radical ( ·OH), able to destroy recalcitrant pollutants in water. Pharmaceuticals considered in this study are aqueous solutions of paracetamol, ibuprofen, and diclofenac at different concentrations 0.1-1 mmol/L, which were treated with irradiation doses from 3 to 15 kGy. The catalytic oxidation of these compounds by gamma irradiation was investigated using hydrogen peroxide (H₂O₂) as a convenient oxidant. Optimization of the main parameters influencing irradiation process, namely irradiation doses, initial concentration and oxidant volume (H₂O₂) were investigated, in the aim to release high degradation efficiency of considered pharmaceuticals. Significant modifications attributed to these parameters appeared in the variation of degradation efficiency, chemical oxygen demand removal (COD) and concentration of radio-induced radicals, confirming them synergistic effect to attempt total mineralization. Pseudo-first-order reaction kinetics could be used to depict the degradation process of these compounds. A sophisticated analytical study was released to quantify the detected radio-induced radicals (electron paramagnetic resonance spectroscopy (EPR) and high performance liquid chromatography (HPLC)). All results showed that this process is effective for the degradation of many pharmaceutical products in aqueous solutions due to strong oxidative properties of generated radicals mainly hydroxyl radical. Furthermore, the addition of an optimal amount of H₂O₂ was efficient to improve the oxidative degradation and contribute to the high performance of this process at very low doses (0.5 and 1 kGy).

Keywords: AOP, COD, hydroxyl radical, EPR, gamma irradiation, HPLC, pharmaceuticals

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567 Redox-Mediated Supramolecular Radical Gel

Authors: Sonam Chorol, Sharvan Kumar, Pritam Mukhopadhyay

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In biology, supramolecular systems require the use of chemical fuels to stay in sustained nonequilibrium steady states termed dissipative self-assembly in contrast to synthetic self-assembly. Biomimicking these natural dynamic systems, some studies have demonstrated artificial self-assembly under nonequilibrium utilizing various forms of energies (fuel) such as chemical, redox, and pH. Naphthalene diimides (NDIs) are well-known organic molecules in supramolecular architectures with high electron affinity and have applications in controlled electron transfer (ET) reactions, etc. Herein, we report the endergonic ET from tetraphenylborate to highly electron-deficient phosphonium NDI²+ dication to generate NDI•+ radical. The formation of radicals was confirmed by UV-Vis-NIR absorption spectroscopy. Electron-donor and electron-acceptor energy levels were calculated from experimental electrochemistry and theoretical DFT analysis. The HOMO of the electron donor locates below the LUMO of the electro-acceptor. This indicates that electron transfer is endergonic (ΔE°ET = negative). The endergonic ET from NaBPh₄ to NDI²+ dication was achieved thermodynamically by the formation of coupled biphenyl product confirmed by GC-MS analysis. NDI molecule bearing octyl phosphonium at the core and H-bond forming imide moieties at the axial position forms a gel. The rheological properties of purified radical ion NDI⦁+ gels were evaluated. The atomic force microscopy studies reveal the formation of large branching-type networks with a maximum height of 70-80 nm. The endergonic ET from NaBPh₄ to NDI²+ dication was used to design the assembly and disassembly redox reaction cycle using reducing (NaBPh₄) and oxidizing agents (Br₂) as chemical fuels. A part of NaBPh₄ is used to drive assembly, while a fraction of the NaBPh₄ is dissipated by forming a useful product. The system goes back to the disassembled NDI²+ dication state with the addition of Br₂. We think bioinspired dissipative self-assembly is the best approach to developing future lifelike materials with autonomous behavior.

Keywords: Ionic-gel, redox-cycle, self-assembly, useful product

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566 Impact of Corn Gluten Hydrolysate on Seedling Growth

Authors: Jyotika Chopra, Dinesh Goyal

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A study was initiated to examine the effects of corn gluten hydrolysate on seedlings growth and its development. Corn gluten is the byproduct of starch industry rich in proteins was hydrolysed by acid and alkali, and the impact of hydrolysate was studied on seed germination of Vigna radiata, Phaseolus vulagris (Fabaceae) and Triticum aestivum and Oryza sativa (Gramineae). For this, the optimum hydrolysis was obtained by 4NHCl and 4M NaOH where insoluble protein in gluten was broken down to glutamic acid, alanine, aspartic acid which was initially confirmed by biuret test, xanthoproteic, solubility and chromatographic tests. The seeds of above families were separately treated with different dilutions of corn gluten hydrolysate ranging from 1-100% to see effects produced by these dilutions on seed germination, plumule, and radical growth. The seedlings were put in the Petri plates and placed in the optimized conditions of temperature (37˚C) and photoperiod of 16:8 hours. The results indicate the plumule of all seeds shows the increase in growth pattern up to 25.75%. Whereas radical shows the increase in growth up to 25.88% till 10% of dilution of corn and wheat gluten hydrolysate with respect to water as blank. Further, there is decrease in growth from 30- 100% of dilutions of both, the hydrolysate indicates the inhibitory effects which unveil about the careful usage of gluten hydrolysate.

Keywords: corn gluten, characterization, hydrolysis, seedling growth

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565 Antioxidant and Anti-Inflammatory Activities of Bioactive Compounds Derived from Thunbergia laurifolia Aqueous Leave Extract

Authors: Marasri Junsi, Sunisa Siripongvutikorn, Chutha Takahashi Yupanqui, Worrapong Usawakesmanee

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Thunbergia laurifolia has been used for folklore medicine purposes and consumed in the form of herbal tea in Thailand since ancient times. To evaluate the bioactive compounds of aqueous leave extract possessed antioxidant and anti-inflammatory activities. The antioxidant activities were examined by total extractable phenolic content (TPC), total extractable flavonoid content (TFC), ABTS radical scavenging, DPPH radical scavenging, FRAP reducing antioxidant power expressed as mg of gallic acid trolox and caffeic acid for the equivalents. Results indicated that the extract had high TPC and antioxidant activities. In addition, the HPLC-DAD analysis of phenolics and flavonoids indicated the presence of caffeic acid and rutin as bioactive compounds. Exposure of cells with the extract using nitric oxide (NO) production in RAW 264.7 murine macrophage cell line induced by lipopolysaccharide (LPS) was significantly reduced NO production and increased cell proliferation. The obtained results demonstrated that the extract contains a high potential to be used as anti-inflammatory and antioxidant substances.

Keywords: Thunbergia laurifolia, anti-inflammatory, antioxidant activities, RAW264.7

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564 Antioxidant Potential and Inhibition of Key Enzymes Linked to Alzheimer's Diseases and Diabetes Mellitus by Monoterpene-Rich Essential Oil from Sideritis Galatica Bornm. Endemic to Turkey

Authors: Gokhan Zengin, Cengiz Sarikurkcu, Abdurrahman Aktumsek, Ramazan Ceylan

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The present study was designated to characterize the essential oil from S. galatica (SGEOs) and evaluate its antioxidant and enzyme inhibitory activities. Antioxidant capacity were tested different methods including free radical scavenging (DPPH, ABTS and NO), reducing power (FRAP and CUPRAC), metal chelating and phosphomolybdenum. Inhibitory activities were analyzed on acetylcholiesterase, butrylcholinesterase, α-amylase and α-glucosidase. SGEOs were chemically analyzed and identified by gas chromatography (GC) and gas chromatography/mass spectrophotometry (GC/MS). 23 components, representing 98.1% of SGEOs were identified. Monoterpene hydrocarbons (74.1%), especially α- (23.0%) and β-pinene (32.2%), were the main constituents in SGEOs. The main sesquiterpene hydrocarbons were β-caryophyllene (16.9%), Germacrene-D (1.2%) and Caryophyllene oxide (1.2%), respectively. Generally, SGEOs has shown moderate free radical, reducing power, metal chelating and enzyme inhibitory activities. These activities related to chemical profile in SGEOs. Our findings supported that the possible utility of SGEOs is a source of natural agents for food, cosmetics or pharmaceutical industries.

Keywords: sideritis galatica, antioxidant, monoterpenes, cholinesterase, anti-diabetic

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563 Investigation of Electrical, Thermal and Structural Properties on Polyacrylonitrile Nano-Fiber

Authors: N. Demirsoy, N. Uçar, A. Önen, N. Kızıldağ, Ö. F. Vurur, O. Eren, İ. Karacan

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Polymer composite nano-fibers including (1, 3 wt %) silver nano-particles have been produced by electrospinning method. Polyacrylonitrile/N,N-dimethylformamide (PAN/DMF) solution has been prepared and the amount of silver nitrate has been adjusted to PAN weight. Silver nano-particles were obtained from reduction of silver ions into silver nano-particles by chemical reduction by hydrazine hydroxide (N2H5OH). The different amount of silver salt was loaded into polymer matrix to obtain polyacrylonitrile composite nano-fiber containing silver nano-particles. The effect of the amount of silver nano-particles on the properties of composite nano-fiber web was investigated. Electrical conductivity, mechanical properties, thermal properties were examined by Microtest LCR Meter 6370 (0.01 mΩ-100 MΩ), tensile tester, differential scanning calorimeter DSC (Q10) and SEM, respectively. Also, antimicrobial efficiency test (ASTM E2149-10) was done against Staphylococcus aureus bacteria. It has been seen that breaking strength, conductivity, antimicrobial effect, enthalpy during cyclization increase by use of silver nano-particles while the diameter of nano-fiber decreases.

Keywords: composite polyacrylonitrile nanofiber, electrical conductivity, electrospinning, mechanical properties, thermal properties, silver nanoparticles

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562 Adopting the Transition Management Model as a Tool for Sustainable Groundwater Management in Nigeria

Authors: Ali Bakari Mohammed

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Transitioning is a continuous process of radical change in a society which involves co-evolution of institutional, technological, socio-cultural, and ecological developments at different scales and levels. Transition management model is a methodology that influences structural change of complex systems over a period (0-30 years) by experimenting and implementing new techniques. A transition management in the context of groundwater is a radical change from the current operate and control system to a next generation integrated and sustainable system that takes into account quality protection and sustained supply into the future. This study evaluates the transition management model in adopting it as a viable tool for the attainment of sustainable groundwater management. The outcome of the evaluation shows that there are three levels (strategic, tactical and operational) of operating the transition management model. At the strategic level, long-term goals for sustainable groundwater management are formulated, at the tactical level activities such as inter institutional networking, negotiation, planning and financing are carried out, and at the operational level, transition experiments and strategic niche management are carried out at the societal level. Overall, different actors and set of activities are required to partake at each management level. The outcome of this paper will provide basis for the implementation of the Sustainable Development Goal (SDG) 6 in Nigeria.

Keywords: transition management, groundwater, sustainable management, tool, Nigeria

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561 Preparation, Structure, and Properties of Hydroxyl Containing Acrylate Monomer Grafted Silk Fabrics by HRP-Catalyzed ATRP Method

Authors: Tieling Xing, Jinqiu Yang, Guoqiang Chen

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It is environmentally friendly to use horseradish peroxidase (HRP) instead of the traditional transition metal catalyst for the catalyst of atom transfer radical polymerization (ATRP). Silk fabrics were successfully grafted with hydroxyl-containing acrylate monomer to improve its crease resistance by HRP-catalyzed ATRP method. Taking grafting yield as the evaluation index, single factor tests revealed that the optimum grafting reaction condition was as follow: monomer mass fraction 120-210%(o.w.f), HRP concentration 360-480U/mL, molar ratio of HRP to NaAsc 1:150, reaction temperature 50-60℃, reaction time 24h. Raman spectra showed hydroxyl-containing acrylate monomer were successfully grafted on silk fabrics. SEM figures indicated the surface of grafted silk became rougher, and graft copolymer was distributed evenly on the surface of silk fiber. The crease-resistant recovery property of grafted silk fabric was greatly improved, especially in wet crease recovery angle. The result showed hydroxyl-containing acrylate monomer can be successfully grafted onto silk fabric based on HRP-catalyzed ATRP method.

Keywords: atom transfer radical polymerization, catalysis, horseradish peroxidase, hydroxyl-containing acrylate monomer

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560 Antimicrobial, Antioxidant and Free Radical Scavenging Activities of Essential Oils Extracted from Six Eucalyptus Species

Authors: Sanaa K. Bardaweel, Mohammad M. Hudaib, Khaled A. Tawaha, Rasha M. Bashatwah

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Eucalyptus species are well reputed for their traditional use in Asia as well as in other parts of the world; therefore, the present study was designed to investigate the antimicrobial and antioxidant activities associated with essential oils from different Eucalyptus species. Essential oils from the leaves of six Eucalyptus species, including: Eucalyptus woodwardi, Eucalyptus stricklandii, Eucalyptus salubris, Eucalyptus sargentii, Eucalyptus torquata and Eucalyptus wandoo were separated by hydrodistillation and dried over anhydrous sodium sulphate. DPPH, ferric reducing antioxidant power, and hydroxyl radical scavenging activity assays were carried out to evaluate the antioxidant potential of the oils. The results indicate that examined oils exhibit substantial antioxidant activities relative to ascorbic acid. Previously, these oils were evaluated for their antimicrobial activities, against wide range of bacterial and fungal strains, and they were shown to possess significant antimicrobial activities. In this study, further investigation into the growth kinetics of oil-treated microbial cultures was conducted. The results clearly demonstrate that the microbial growth was markedly inhibited when treated with sub-MIC concentrations of the oils. Taken together, the results obtained indicate a high potential of the examined essential oils as bioactive oils, for nutraceutical and medical applications, possessing significant antioxidant and anti microbial activities.

Keywords: antimicrobial, antioxidants, essential (volatile) oil, Eucalyptus

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559 In vitro Antioxidant, Anticancer Properties and Probiotic Characteristics of Selected Lactic Acid Bacteria Strains

Authors: M. G. Shehata, S. A. El Sohaimy, Marwa M. Abu-Serie, Nourhan M. Abd El-Aziz

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Probiotic strains can potentially be used as bio-preservatives and functional food supplement. Eight lactic acid bacteria strains (LAB) Lactobacillus brevis NRRL B-4527; Streptococcus thermophilus BLM 58; Pediococcusacidilactici ATCC 8042; Lactobacillus rhamnosus CCUG 1452; Lactobacillus curvatus ATCC 51436; Lactococcuslactis sub sp. lactisDSM 20481; Lactobacillus plantarum DMSZ 20079 and Lactobacillus plantarumTF103 were selected to screen the antioxidant, anticancer potential and probiotic properties. LAB strains exhibited good probiotic, antioxidant properties and showed antagonistic activity against food-borne pathogenic (Bacillus subtilis DB 100 host; Candida albicans ATCCMYA-2876; Clostridium botulinum ATCC 3584; Escherichia coli BA 12296; Klebsiellapneumoniae ATCC12296; Salmonella senftenberg ATCC 8400 and Staphylococcus aureus NCTC 10788). Further, in vitro probiotic properties of eight strains displayed excellent acid tolerance, bile tolerance, simulated gastrointestinal juice tolerance, in vitro adhesion ability for HT-29 cell line. The antioxidant effect of intracellular and cell-free extract of lactic acid bacteria strains was evaluated by various antioxidant assays, namely, resistance to hydrogen peroxide, DPPH radical scavenging, ABTS radical scavenging, and hydroxyl radical scavenging (HRS). The results showed that intracellular and cell-free supernatant of S. Thermophilus BLM 58, L. lactissubsp.lactis DSM 20481, P. acidilactici ATCC 8042, L. brevis NRRL B-4527 strains possess excellent antioxidant capacity. The intracellular of S. Thermophilus BLM 58 and P. acidilactici ATCC 8042 also showed excellent anticancer activity against Caco-2, MCF-7, HepG-2, and PC-3. Antioxidative property of selected lactic acid bacteria strains would be useful in the functional food manufacturing industry. They could beneficially affect the consumer by providing dietary source of antioxidants.

Keywords: anticancer activity, antioxidant activity, functional food, lactic acid bacteria, probiotic

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558 Peach as a Potential Functional Food: Biological Activity and Important Phenolic Compound Source

Authors: Luís R. Silva, Catarina Bento, Ana C. Gonçalves, Fábio Jesus, Branca M. Silva

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Nowadays, the general population is more and more concerned about nutrition and the health implications of an unbalanced diet. Current knowledge regarding the health benefits and antioxidant properties of certain foods such as fruits and vegetables has gained the interest of both the general public and scientific community. Peach (Prunus persica (L.) Batsch) is one of the most consumed fruits worldwide, with low sugar contents and a broad range of nutrients essential to the normal functioning of the body. Six different peach cultivars from the Fundão region in Portugal were evaluated regarding their phenolic composition by LC-DAD and biological activity. The prepared extracts’ capacity to scavenge free-radicals was tested through the stable free radical DPPH• and nitric oxide (•NO). Additionally, antidiabetic potential and protective effects against peroxyl radical (ROO•) induced damage to erythrocytes were also tested. LC-DAD analysis allowed the identification of 17 phenolic compounds, among which 5-O-caffeoylquinic acids and 3-O-caffeoylquinic acids are pointed out as the most abundant. Regarding the antioxidant activity, all cultivars displayed concentration-dependent free-radical scavenging activity against both nitrogen species and DPPH•. In respect to α-glucosidase inhibitory activity, Royal Magister and Royal Glory presented the highest inhibitory activity (IC50 = 11.7 ± 1.4 and 17.1 ± 1.7 μg/mL, respectively), nevertheless all six cultivars presented higher activity than the control acarbose. As for the protective effect of Royal Lu extract on the oxidative damage induced in erythrocytes by ROO•, the results were quite promising showing inhibition IC50 values of 110.0 ± 4.5 μg/mL and 83.8 ± 6.5 μg/mL for hemolysis and hemoglobin oxidation, respectively. The demonstrated activity is of course associated to the peaches’ phenolic profile, rich in phenolic acids and flavonoids with high hydrogen donating capacity. These compounds have great industrial interest for the manufacturing of natural products. The following step would naturally be the extraction and isolation from the plant tissues and large-scale production through biotechnology techniques.

Keywords: antioxidants, functional food, phenolic compounds, peach

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557 The Effect of Different Concentrations of Extracting Solvent on the Polyphenolic Content and Antioxidant Activity of Gynura procumbens Leaves

Authors: Kam Wen Hang, Tan Kee Teng, Huang Poh Ching, Chia Kai Xiang, H. V. Annegowda, H. S. Naveen Kumar

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Gynura procumbens (G. procumbens) leaves, commonly known as ‘sambung nyawa’ in Malaysia is a well-known medicinal plant commonly used as folk medicines in controlling blood glucose, cholesterol level as well as treating cancer. These medicinal properties were believed to be related to the polyphenolic content present in G. procumbens extract, therefore optimization of its extraction process is vital to obtain highest possible antioxidant activities. The current study was conducted to investigate the effect of different concentrations of extracting solvent (ethanol) on the amount of polyphenolic content and antioxidant activities of G. procumbens leaf extract. The concentrations of ethanol used were 30-70%, with the temperature and time kept constant at 50°C and 30 minutes, respectively using ultrasound-assisted extraction. The polyphenolic content of these extracts were quantified by Folin-Ciocalteu colorimetric method and results were expressed as milligram gallic acid equivalent (mg GAE)/g. Phosphomolybdenum method and 1, 1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging assays were used to investigate the antioxidant properties of the extract and the results were expressed as milligram ascorbic acid equivalent (mg AAE)/g and effective concentration (EC50) respectively. Among the three different (30%, 50% and 70%) concentrations of ethanol studied, the 50% ethanolic extract showed total phenolic content of 31.565 ± 0.344 mg GAE/g and total antioxidant activity of 78.839 ± 0.199 mg AAE/g while 30% ethanolic extract showed 29.214 ± 0.645 mg GAE/g and 70.701 ± 1.394 mg AAE/g, respectively. With respect to DPPH radical scavenging assay, 50% ethanolic extract had exhibited slightly lower EC50 (314.3 ± 4.0 μg/ml) values compared to 30% ethanol extract (340.4 ± 5.3 μg/ml). Out of all the tested extracts, 70% ethanolic extract exhibited significantly (p< 0.05) highest total phenolic content (38.000 ± 1.009 mg GAE/g), total antioxidant capacity (95.874 ± 2.422 mg AAE/g) and demonstrated the lowest EC50 in DPPH assay (244.2 ± 5.9 μg/ml). An excellent correlations were drawn between total phenolic content, total antioxidant capacity and DPPH radical scavenging activity (R2 = 0.949 and R2 = 0.978, respectively). It was concluded from this study that, 70% ethanol should be used as the optimal polarity solvent to obtain G. procumbens leaf extract with maximum polyphenolic content with antioxidant properties.

Keywords: antioxidant activity, DPPH assay, Gynura procumbens, phenolic compounds

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556 Kinetic Study of Municipal Plastic Waste

Authors: Laura Salvia Diaz Silvarrey, Anh Phan

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Municipal Plastic Waste (MPW) comprises a mixture of thermoplastics such as high and low density polyethylene (HDPE and LDPE), polypropylene (PP), polystyrene (PS) and polyethylene terephthalate (PET). Recycling rate of these plastics is low, e.g. only 27% in 2013. The remains were incinerated or disposed in landfills. As MPW generation increases approximately 5% per annum, MPW management technologies have to be developed to comply with legislation . Pyrolysis, thermochemical decomposition, provides an excellent alternative to convert MPW into valuable resources like fuels and chemicals. Most studies on waste plastic kinetics only focused on HDPE and LDPE with a simple assumption of first order decomposition, which is not the real reaction mechanism. The aim of this study was to develop a kinetic study for each of the polymers in the MPW mixture using thermogravimetric analysis (TGA) over a range of heating rates (5, 10, 20 and 40°C/min) in N2 atmosphere and sample size of 1 – 4mm. A model-free kinetic method was applied to quantify the activation energy at each level of conversion. Kissinger–Akahira–Sunose (KAS) and Flynn–Wall–Ozawa (FWO) equations jointly with Master Plots confirmed that the activation energy was not constant along all the reaction for all the five plastic studied, showing that MPW decomposed through a complex mechanism and not by first-order kinetics. Master plots confirmed that MPW decomposed following a random scission mechanism at conversions above 40%. According to the random scission mechanism, different radicals are formed along the backbone producing the cleavage of bonds by chain scission into molecules of different lengths. The cleavage of bonds during random scission follows first-order kinetics and it is related with the conversion. When a bond is broken one part of the initial molecule becomes an unsaturated one and the other a terminal free radical. The latter can react with hydrogen from and adjacent carbon releasing another free radical and a saturated molecule or reacting with another free radical and forming an alkane. Not every time a bonds is broken a molecule is evaporated. At early stages of the reaction (conversion and temperature below 40% and 300°C), most products are not short enough to evaporate. Only at higher degrees of conversion most of cleavage of bonds releases molecules small enough to evaporate.

Keywords: kinetic, municipal plastic waste, pyrolysis, random scission

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555 Nanoemulsion Formulation of Ethanolic Extracts of Propolis and Its Antioxidant Activity

Authors: Rachmat Mauludin, Dita Sasri Primaviri, Irda Fidrianny

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Propolis contains several antioxidant compounds which can be used in topical application to protect skin against free radical, prevent skin cancer and skin aging. Previous study showed that 70% ethanolic extract of propolis (EEP) provided the greatest antioxidant activity. Since EEP has very small solubility in water, the extract was prepared in nanoemulsion (NE). Nanoemulsion is chosen as cosmetic dosage forms according to its properties namely to decrease the risk of skin’s irritation, increase penetration, prolong its time to remain in our skin, and improve stability. Propolis was extracted using reflux methods and concentrated using rotavapor. EEP was characterized with several tests such as phytochemical screening, density, and antioxidant activity using DPPH method. Optimation of total surfactant, co-surfactant, oil, and amount of EEP that can be included in NE were required to get the best NE formulation. The evaluations included to organoleptic observation, globul size, polydispersity index, morphology using TEM, viscosity, pH, centrifuge, stability, Freeze and Thaw test, radical scavenging activity using DPPH method, and primary irritation test. The yield extracts was 11.12% from raw propolis contained of steroid/triterpenoid, flavonoid, and saponin based on phytochemical screening. EEP had the value of DPPH scavenging activity 61.14% and IC50 0.41629 ppm. The best NE formulation consisted of 26.25% Kolliphor RH40; 8.75% glycerine; 5% rice bran oil; and 3% EEP. NE was transparant, had globul size of 21.9 nm; polydispersity index of 0.338; and pH of 5.67. Based on TEM morphology, NE was almost spherical and has particle size below 50 nm. NE propolis revealed to be physically stable after stability test within 63 days at 25oC, centrifuged for 30 mins at 13.000 rpm, and passed 6 cycles of Freeze and Thaw test without separated. NE propolis reduced 58% of free radical DPPH similar to antioxidant activity of the original extracts. Antioxidant activity of NE propolis is relatively stable after stored for 6 weeks. NE Propolis was proven to be safe by primary irritation test with the value of primary irritation index (OECD) was 0. The best formulation for NE propolis contained of 26.25% Kolliphor RH40; 8.75% glycerine; 5% rice bran oil; and 3% EEP with globul size of 21.9 nm and polydispersity index of 0.338. NE propolis was stable and had antioxidant activity similar to EEP.

Keywords: propolis, antioxidant, nanoemulsion, irritation test

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554 A Thermodynamic Study of Parameters that Affect the Nitration of Glycerol with Nitric Acid

Authors: Erna Astuti, Supranto, Rochmadi, Agus Prasetya

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Biodiesel production from vegetable oil will produce glycerol as by-product about 10% of the biodiesel production. The amount of glycerol that was produced needed alternative way to handling immediately so as to not become the waste that polluted environment. One of the solutions was to process glycerol to polyglycidyl nitrate (PGN). PGN is synthesized from glycerol by three-step reactions i.e. nitration of glycerol, cyclization of 13- dinitroglycerine and polymerization of glycosyl nitrate. Optimum condition of nitration of glycerol with nitric acid has not been known. Thermodynamic feasibility should be done before run experiments in the laboratory. The aim of this study was to determine the parameters those affect nitration of glycerol and nitric acid and chose the operation condition. Many parameters were simulated to verify its possibility to experiment under conditions which would get the highest conversion of 1, 3-dinitroglycerine and which was the ideal condition to get it. The parameters that need to be studied to obtain the highest conversion of 1, 3-dinitroglycerine were mol ratio of nitric acid/glycerol, reaction temperature, mol ratio of glycerol/dichloromethane and pressure. The highest conversion was obtained in the range of mol ratio of nitric acid /glycerol between 2/1 – 5/1, reaction temperature of 5-25o C and pressure of 1 atm. The parameters that need to be studied further to obtain the highest conversion of 1.3 DNG are mol ratio of nitric acid/glycerol and reaction temperature.

Keywords: Nitration, glycerol, thermodynamic, optimum condition

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553 Benzoxaboralone: A Boronic Acid with High Oxidative Stability and Utility in Biological Contexts

Authors: Brian J. Graham, Ronald T. Raines

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The presence of a nearly vacant p orbital on boron endows boronic acids with unique abilities as a catalyst and ligand. An organocatalytic process has been developed for the conversion of biomass-derived sugars to 5-hydroxymethylfurfural, which is a platform chemical. Specifically, 2-carboxyphenylboronic acid (2-CPBA) has been shown to be an optimal catalyst for this process, promoting the desired transformation in the absence of metals. The attributes of 2-CPBA as a catalyst led to additional investigations of its structure and reactivity. 2-CPBA was found to exist as a cyclized benzoxaborolone adduct rather than a free carboxylic acid. This cyclization has profound consequences for the oxidative stability of the boronic acid. Stereoelectronic effects within the oxaborolone ring destabilize the oxidation transition state by reducing electron donation from the cyclic oxygen to the developing p orbital on boron. That leads to a 10,000-fold increase in oxidative stability while maintaining the normal reactivity of boronic acids toward diols (e.g., carbohydrates) and nucleophiles in proteins while also presenting numerous hydrogen-bond accepting and donating groups. Thus, benzoxaborolones are useful in catalysis, chemical biology, medicinal chemistry, and allied fields.

Keywords: bioisosteres, boronic acid, catalysis, oxidative stability, pharmacophore, stereoelectronic effects

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552 Going beyond Stakeholder Participation

Authors: Florian Engel

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Only with a radical change to an intrinsically motivated project team, through giving the employees the freedom for autonomy, mastery and purpose, it is then possible to develop excellent products. With these changes, combined with using a rapid application development approach, the group of users serves as an important indicator to test the market needs, rather than only as the stakeholders for requirements.

Keywords: intrinsic motivation, requirements elicitation, self-directed work, stakeholder participation

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551 Natural Honey and Effect on the Activity of the Cells

Authors: Abujnah Dukali

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Natural honey was assessed in cell culture system for its anticancer activity. Human leukemic cell line HL 60 was treated with honey and cultured for 5 days and cytotoxicity was calculated by MTT assay. Honey showed cytotoxicity with CC50 value of 174.20 µg/ml. Radical modulation activities was assessed by lipid peroxidation assay using egg lecithin. Honey showed antioxidant activity with EC50 value of 159.73 µg/ml. In addition, treatment with HL60 cells also resulted in nuclear DNA fragmentation, as seen in agarose gel electrophoresis. This is a hallmark of cells undergoing apoptosis. Confirmation of apoptosis was performed by staining the cells with Annexin V and FACS analysis. Apoptosis is an active, genetically regulated disassembly of the cell form within. Disassembly creates changes in the phospholipid content of the cytoplasmic membrane outer leaflet. Phosphatidylserine (PS) is translocated from the inner to the outer surface of the cell for phagocytic cell recognition. The human anticoagulant, annexin V, is a Ca2+-dependent phospholipid protein with a high affinity for PS. Annexin V labeled with fluorescein can identify apoptotic cells in the population It is a confirmatory test for apoptosis. Annexin V-positive cells were defined as apoptotic cells. Since honey shows both antioxidant activity and cytotoxicity at almost the same concentration, it can prevent the free radical induced cancer as prophylactic agent and kill the cancer cells by apoptotic process as a chemotherapeutic agent. Everyday intake of honey can prevent the cancer induction.

Keywords: anticancer, cells, DNA, honey

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550 Antioxidant Activity Of Gracilaria Fisheri Extract

Authors: Paam Bidaya

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The red seaweed Gracilaria fisheri, widely distributed along Thailand's southern coastlines, has been discovered to be edible. Sulfated polysaccharides from G. fisheri were extracted in low-temperature (25 °C) water. Seaweed polysaccharides (SPs) have been shown to have various advantageous biological effects. This study aims to investigate total phenolic content and antioxidant capacity of G. fisheri extract. The total phenolic content of G. fisheri extract was determined using Folin-Cioucalteu method and calculated as gallic acid equivalents (GAE). The antioxidant activity of G. fisheri extract was performed via 2, 2-diphenyl-1- picrylhydrazyl (DPPH) free radical scavenging assay and 2,2’-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical scavenging capacity assays. The findings exhibited a strong correlation between antioxidant activity and the total phenol contents. In addition, DPPH and ABTS assays showed that G. fisheri extract showed antioxidant activities as a concentration-dependent manner. The IC50 values of G. fisheri extract were 902.19 μg/mL ± 0.785 and 727.98 μg/mL ± 0.822 for DPPH and ABTS, respectively. Vitamin C was used as a positive control in DPPH assay, while Trolox was used as a positive control in ABTS assay. To conclude, G. fisheri extract consists of a high amount of total phenolic content, which exhibit a significant antioxidant activity. However, further investigation regarding antioxidant activity should be performed in order to identify the mechanism of Gracilaria fisheri action.

Keywords: ABTS assay, DPPH assay, sulfated polysaccharides, total phenolic content

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549 Preparation and Antioxidant Activity of Heterocyclic Indole Derivatives

Authors: Tunca Gul Altuntas, Aziz Baydar, Cemre Acar, Sezen Yılmaz, Tulay Coban

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Free radicals, which are generated in many bioorganic redox processes, play a role in the pathogenesis of several diseases including cancer, arthritis, hemorrhagic shock, inflammatory, cardiovascular, neurodegenerative diseases and age-related degenerative brain diseases. Exposures of normal cell to free radical damages several structures, oxidizes nucleic acids, proteins, lipids, or DNA. Compounds interfere with the action of reactive oxygen species might be useful in prevention and treatment of these pathologies. A series of indole compounds containing piperazine ring were synthesized. Coupling of indole-2-carboxylic acid with monosubstituted piperazines was accomplished with 1,1’-carbonyldiimidazole (CDI) in a good yield. The structures of prepared compounds were verified in good agreement with their 1H NMR (nuclear magnetic resonance), MS (mass spectrophotometry), and IR (infrared spectrophotometry) characteristics. In this work, all synthetized indole derivatives were screened in vitro for their antioxidative potential against vitamin E (α-tocopherol) using different antioxidant assays such as superoxide anion formation, lipid peroxidation levels in rat liver, and 2,2-diphenyl-1-picrylhydrazyl (DPPH) stable radical scavenging activity. The synthesized compounds showed various levels of inhibition compared to vitamin E. This may give promising results for the development of new antioxidant agents.

Keywords: antioxidant, indoles, piperazines, reactive oxygen species

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548 Transformation of Glycals to Chiral Fused Aromatic Cores via Annulative π-Extension Reaction with Arynes

Authors: Nazar Hussain, Debaraj Mukherjee

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Carbohydrate-derived chiral intermediates which contain arrays of defined stereocenters have found enormous applications in organic synthesis due to their inherent functional group, stereochemical and structural diversities as well as their ready availability. Stereodiversity of these classes of molecules has motivated synthetic organic chemistry over the years. One major challenge is control of relative configuration during construction of acyclic fragments. Here, we show that The Diels Alder addition of arynes to appropriately substituted vinyl/aryl glycals followed by π-extension via pyran ring opening smoothly furnished meta-disubstituted fused aromatic cores containing a stereo-defined orthogonally protected chiral side chain. The method is broad in terms of aryl homologation affording benzene, naphthalene, and phenanthrene derivatives. Base-induced deprotonation followed by cleavage of the allylic C-O bond appears to be the crucial steps leading to the development of aromaticity, which is the driving force behind the annulative π-extension process. The present protocol can be used for the synthesis of meta-disubstituted naphthalene aldehydes and substrates for aldolases.

Keywords: vinyl/C-2 aryl glycal, arynes, cyclization, ring opening

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547 Phytochemical Screening and in vitro Antibacterial and Antioxidant Potential of Microalgal Strain, Cymbella

Authors: S. Beekrum, B. Odhav, R. Lalloo, E. O. Amonsou

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Marine microalgae are rich sources of the novel and biologically active metabolites; therefore, they may be used in the food industry as natural food ingredients and functional foods. They have several biological applications related with health benefits, among others. In the past decades, food scientists have been searching for natural alternatives to replace synthetic antioxidants. The use of synthetic antioxidants has decreased due to their suspected activity as promoters of carcinogenesis, as well as consumer rejection of synthetic food additives. The aim of the study focused on screening of phytochemicals from Cymbella biomass extracts, and to examine the in vitro antioxidant and antimicrobial potential. Cymbella biomass was obtained from CSIR (South Africa), and four different solvents namely methanol, acetone, n-hexane and water were used for extraction. To take into account different antioxidant mechanisms, seven different antioxidant assays were carried out. These include free radical scavenging (DPPH assay), Trolox equivalent antioxidant capacity (TEAC assay), radical cation (ABTS assay), superoxide anion radical scavenging, reducing power, determination of total phenolic compounds and determination of total flavonoid content. The total content of phenol and flavonoid in extracts were determined as gallic acid equivalent, and as rutin equivalent, respectively. The in vitro antimicrobial effect of extracts were tested against some pathogens (Staphylococcus aureus, Listeria monocytogenes, Bacillus subtilis, Salmonella enteritidis, Escherichia coli, Pseudomonas aeruginosa and Candida albicans), using the disc diffusion assay. Qualitative analyses of phytochemicals were conducted by chemical tests to screen for the presence of tannins, flavonoids, terpenoids, phenols, steroids, saponins, glycosides and alkaloids. The present investigation revealed that all extracts showed relatively strong antibacterial activity against most of the tested bacteria. The methanolic extract of the biomass contained a significantly high phenolic content of 111.46 mg GAE/g, and the hexane extract contained 65.279 mg GAE/g. Results of the DPPH assay showed that the biomass contained strong antioxidant capacity, 79% in the methanolic extract and 85% in the hexane extract. Extracts have displayed effective reducing power and superoxide anion radical scavenging. Results of this study have highlighted potential antioxidant activity in the methanol and hexane extracts. The obtained results of the phytochemical screening showed the presence of terpenoids, flavonoids, phenols and saponins. The use of Cymbella as a natural antioxidant source and a potential source of antibacterial compounds and phytochemicals in the food industry appears promising and should be investigated further.

Keywords: antioxidants, antimicrobial, Cymbella, microalgae, phytochemicals

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546 Antioxidant Properties, Ascorbic Acid and Total Carotenoids Values of Sweet and Hot Red Pepper Paste: A Traditional Food in Turkish Diet

Authors: Kubra Sayin, Derya Arslan

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Red pepper (Capsicum annum L.) has long been recognized as a good source of antioxidants, being rich in ascorbic acid and other phytochemicals. In Turkish cuisine red pepper is sometimes consumed raw in salads and baked as a garnish, but its most wide consumption type is red pepper paste. The processing of red pepper into pepper paste includes various thermal treatment steps such as heating and pasteurizing. There are reports demonstrating an enhancement or reduction in antioxidant activity of vegetables after thermal treatment. So this study was conducted to investigate the total phenolics, ascorbic acid and total carotenoids as well as free radical scavenging activity of raw red pepper and various red pepper pastes obtainable on the market. The samples were analyzed for radical-scavenging activity (RSA) and total polyphenol (TP) content using 1,1-diphenyl-2-picrylhydrazyl (DPPH) and Folin-Ciocalteu methods, respectively. They were also evaluated for ascorbic acid content (AsA) by HPLC. Total carotenoids content was determined spectrophotometrically. Results suggest that there is no significant (P > 0.05) difference in RSA, TP, AsA and total carotenoids content between various red pepper paste products. However, red pepper paste showed marked differences (P < 0.05) in the RSA, TP and AsA contents compared with raw red pepper. It is concluded that the red pepper paste, that has a wide range of consumption in Turkish cuisine, presents a good dose of phenolic compounds and antioxidant capacity and it should be regarded as a functional food.

Keywords: red pepper paste, antioxidant properties, total carotenoids, total phenolics

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545 Caffeic Acid in Cosmetic Formulations: An Innovative Assessment

Authors: Caroline M. Spagnol, Vera L. B. Isaac, Marcos A. Corrêa, Hérida R. N. Salgado

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Phenolic compounds are abundant in the Brazilian plant kingdom and they are part of a large and complex group of organic substances. Cinnamic acids are part of this group of organic compounds, and caffeic acid (CA) is one of its representatives. Antioxidants are compounds which act as free radical scavengers and, in other cases, such as metal chelators, both in the initiation stage and the propagation of oxidative process. The tyrosinase, polyphenol oxidase, is an enzyme that acts at various stages of melanin biosynthesis within the melanocytes and is considered a key molecule in this process. Some phenolic compounds exhibit inhibitory effects on melanogenesis by inhibiting the tyrosinase enzymatic activity and therefore has been the subject of studies. However, few studies have reported the effectiveness of these products and their safety. Objectives: To assess the inhibitory activity of tyrosinase, the antioxidant activity of CA and its cytotoxic potential. The method to evaluate the inhibitory activity of tyrosinase aims to assess the reduction transformation of L-dopa into dopaquinone reactions catalyzed by the enzyme. For evaluating the antioxidant activity was used the analytical methodology of DPPH radical inhibition. The cytotoxicity evaluation was carried out using the MTT method (3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide), a colorimetric assay which determines the amount of insoluble violet crystals formed by the reduction of MTT in the mitochondria of living cells. Based on the results obtained during the study, CA has low activity as a depigmenting agent. However, it is a more potent antioxidant than ascorbic acid (AA), since a lower amount of CA is sufficient to inhibit 50% of DPPH radical. The results are promising since CA concentration that promoted 50% toxicity in HepG2 cells (IC50=781.8 μg/mL) is approximately 330 to 400 times greater than the concentration required to inhibit 50% of DPPH (IC50 DPPH= 2.39 μg/mL) and ABTS (IC50 ABTS= 1.96 μg/mL) radicals scavenging activity, respectively. The maximum concentration of caffeic acid tested (1140 mg /mL) did not reach 50% of cell death in HaCat cells. Thus, it was concluded that the caffeic acid does not cause toxicity in HepG2 and HaCat cells in the concentrations required to promote antioxidant activity in vitro, and it can be applied in topical products.

Keywords: caffeic acid, antioxidant, cytotoxicity, cosmetic

Procedia PDF Downloads 356
544 4(3H)-Quinazolinone Derivatives' Synthesis and Evaluation as Antimalarial and Anti-Leishmanial Agents

Authors: Alemu Tadesse Feroche

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In this study, some 2, 3 distributed quinazoline -4 (3H) - one derivative were synthesized using a three-step synthetic route. They were obtained in a good yield (59.5-85%) by applying different chemical reactions like cyclization and condensation reactions. The chemical structure of the final compounds was also verified by spectroscopic methods (IR, ¹HNMR) and elemental microanalysis. The in vivo antimalarial activity of these compounds on P. berghei infected mice was found to be moderate to high at an oral dose of 0.04846 mmol/kg /day. This is equal to 25 mg/kg of chloroquine phosphate, which causes 100% inhibition of the parasite. It is worth mentioning that most active compounds (E) -3 Phenyl -2- [2- (pyridine -4- yl) vinyl] -4 (3H) -quinazolinone IVa (64.02%, (E)-2-[2-(4 - Hydroxy-3 - methoxystyryl) - vinyl) -3 - phenyl -4 (3H ) - quinazolinone IVc (77.25%) and (E)-2 –[2 –(Pyridin -4-yl) –vinyl] -3 phenenylamine -4(3H) quinazolinone IVe (73.54%) showed a dose-dependent increase in present suppression in antimalarial activities. Furthermore, the synthesized compounds were screened for their in vitro antileishmanial activity against L. aethiopica isolate (CL/039/09). All tested compounds (IVa (0.03766 ug/ml), IVb (0.00538 ug/ml, IVc (0.00412 ug/ml, IVd (0.00110 ug/ml), IVe (0.03017 ug/ml) and IVf (0.03894 ug/ml)) showed excellent potency that is much better than amphotericin B (IC50 = 0,04359 ug/ml). The results of acute toxicity indicated that all test compounds (IVa –IVf) proved to be nontoxic and well tolerated by the experimental animals up to 300 mg/kg in oral and 140 mg/kg in parental studies.

Keywords: 4(3H)-quinazolinone, in vivo antimalarial activity, in vitro antileishmanial activity, acute toxicity

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543 ¹⁸F-FDG PET/CT Impact on Staging of Pancreatic Cancer

Authors: Jiri Kysucan, Dusan Klos, Katherine Vomackova, Pavel Koranda, Martin Lovecek, Cestmir Neoral, Roman Havlik

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Aim: The prognosis of patients with pancreatic cancer is poor. The median of survival after establishing diagnosis is 3-11 months without surgical treatment, 13-20 months with surgical treatment depending on the disease stage, 5-year survival is less than 5%. Radical surgical resection remains the only hope of curing the disease. Early diagnosis with valid establishment of tumor resectability is, therefore, the most important aim for patients with pancreatic cancer. The aim of the work is to evaluate the contribution and define the role of 18F-FDG PET/CT in preoperative staging. Material and Methods: In 195 patients (103 males, 92 females, median age 66,7 years, 32-88 years) with a suspect pancreatic lesion, as part of the standard preoperative staging, in addition to standard examination methods (ultrasonography, contrast spiral CT, endoscopic ultrasonography, endoscopic ultrasonographic biopsy), a hybrid 18F-FDG PET/CT was performed. All PET/CT findings were subsequently compared with standard staging (CT, EUS, EUS FNA), with peroperative findings and definitive histology in the operated patients as reference standards. Interpretation defined the extent of the tumor according to TNM classification. Limitations of resectability were local advancement (T4) and presence of distant metastases (M1). Results: PET/CT was performed in a total of 195 patients with a suspect pancreatic lesion. In 153 patients, pancreatic carcinoma was confirmed and of these patients, 72 were not indicated for radical surgical procedure due to local inoperability or generalization of the disease. The sensitivity of PET/CT in detecting the primary lesion was 92.2%, specificity was 90.5%. A false negative finding in 12 patients, a false positive finding was seen in 4 cases, positive predictive value (PPV) 97.2%, negative predictive value (NPV) 76,0%. In evaluating regional lymph nodes, sensitivity was 51.9%, specificity 58.3%, PPV 58,3%, NPV 51.9%. In detecting distant metastases, PET/CT reached a sensitivity of 82.8%, specificity was 97.8%, PPV 96.9%, NPV 87.0%. PET/CT found distant metastases in 12 patients, which were not detected by standard methods. In 15 patients (15.6%) with potentially radically resectable findings, the procedure was contraindicated based on PET/CT findings and the treatment strategy was changed. Conclusion: PET/CT is a highly sensitive and specific method useful in preoperative staging of pancreatic cancer. It improves the selection of patients for radical surgical procedures, who can benefit from it and decreases the number of incorrectly indicated operations.

Keywords: cancer, PET/CT, staging, surgery

Procedia PDF Downloads 225