Search results for: biologically active

Authors: Mahdi Alshamasin, Riad Al-Kasasbeh, Nikolay Korenevskiy

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We apply mathematical models for the interaction of the internal and biologically active points of meridian structures. Amongst the diseases for which reflex diagnostics are effective are those of the stomach disease. It is shown that use of fuzzy logic decision-making yields good results for the prediction and early diagnosis of gastrointestinal tract diseases, depending on the reaction energy of biologically active points (acupuncture points). It is shown that good results for the prediction and early diagnosis of diseases from the reaction energy of biologically active points (acupuncture points) are obtained by using fuzzy logic decision-making.

Keywords: acupuncture points, fuzzy logic, diagnostically important points (DIP), confidence factors, membership functions, stomach diseases

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Authors: I. B. Patel, K. A. Mistry, A. H. Prajapati

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Biologically synthesized colloidal Pd nanoparticles were impregnated on porous aluminium. In this paper, the obtained Pd/Al2O3 catalysts were characterized by XRD, SEM, and TEM. The effects of deposited films on the performances of Pd/Al2O3 in adsorption, reduction, and catalytic reaction of CO2 were investigated. The results showed that the deposited films can remarkably improve the dispersion of active components and enhance the reactivity of Pd/Al2O3 catalyst. The catalytic performance of Pd/Al2O3 in term of surface reaction is also enhanced in terms of sensitivity (SF = 850) obtained through conventional CBD method.

Keywords: palladium nanoparticles, Pd/Al2O3, carbon dioxide, aluminium catalyst

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Authors: Shen Jian, Hu Jie, Ma Jin, Peng Ying Hong, Fang Yi, Liu Wen Hai

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Biologically inspired design inspires inventions and new technologies in the field of engineering by mimicking functions, principles, and structures in the biological domain. To deal with the obstacles of cross-domain knowledge acquisition in the existing biologically inspired design process, functional semantic clustering based on functional feature semantic correlation and environmental constraint clustering composition based on environmental characteristic constraining adaptability are proposed. A knowledge cell clustering algorithm and the corresponding prototype system is developed. Finally, the effectiveness of the method is verified by the visual prosthetic device design.

Keywords: knowledge clustering, knowledge acquisition, knowledge based engineering, knowledge cell, biologically inspired design

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Authors: Neeraj Kumar Mishra, In Su Kim

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The isoindoline, indazole and indole heterocycles are ubiquitous structural motif found in heterocyclic compounds as they exhibit biological and medicinal applications. For example, isoindoline motif is present in molecules that act as endothelin-A receptor antagonists and dipeptidyl peptidase inhibitors. Moreover, isoindoline derivatives are very crucial constituents in the field of materials science as attractive candidates for organic light-emitting devices. However, compounds containing the indazole motif are known to exhibit to a variety of biological activities, such as estrogen receptor, HIV protease inhibition and anti-tumor activity. The prevalence of indazoles and indoles has led to the development of many useful methods for their preparation. Thus, isoindoline, indazole and indole heterocycles can be new candidates for the next generation of pharmaceuticals. Therefore, the development of highly efficient strategies for the formation of these heterocyclic architectures is an area of great interest in organic synthesis. The past years, transition-metal-catalyzed C−H activation followed by annulation reaction has been frequently used as a powerful tool to construct various heterocycles. Herein, we describe our recent achievements about the transition-metal-catalyzed tandem cyclization reactions of N-benzyltriflamides, 1,2-disubstituted arylhydrazines, acetanilides, etc. via C−H bond activation to access the corresponding bioactive heterocylic scaffolds.

Keywords: biologically active, C-H activation, heterocyclic compounds, transition-metal catalysts

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Authors: Youn Young Shim, Ji Hye Kim, Jae Youl Cho, Martin J. T. Reaney

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Flaxseed (Linum usitatissimum L.) is gaining popularity in the food industry as a superfood due to its health-promoting properties. The flax plant synthesizes an array of biologically active cyclic peptides or linusorbs (LOs, a.k.a. cyclolinopeptides) from three or more ribosome-derived precursors. [1–9-NαC]-linusorb B3 and [1–9-NαC]-linusorb B2, suppress immunity, induce apoptosis in human epithelial cancer cell line (Calu-3) cells, and inhibit T-cell proliferation, but the mechanism of LOs action is unknown. Using gene expression analysis in nematode cultures and human cancer cell lines, we have observed that LOs exert their activity, in part, through induction of apoptosis. Specific LOs’ properties include: 1) distribution throughout the body after flaxseed consumption; 2) induce heat shock protein (HSP) 70A production as an indicator of stress and address the issue in Caenorhabditis elegans (exposure of nematode cultures to [1–9-NαC]-linusorb B3 induced a 30% increase in production of the HSP 70A protein); 3) induce apoptosis in Calu-3 cells; and 4) modulate regulatory genes in microarray analysis. These diverse activities indicate that LOs might induce apoptosis in cancer cells or act as versatile platforms to deliver a variety of biologically active molecules for cancer therapy.

Keywords: flaxseed, linusorb, cyclic peptide, orbitides, heat shock protein, apoptosis, anti-cancer

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Authors: Naira Sahakyan, Margarit Petrosyan, Armen Trchounian

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One of the tasks in contemporary biotechnology, pharmacology and other fields of human activities is to obtain biologically active substances from plants. They are very essential in the treatment of many diseases due to their actually high therapeutic value without visible side effects. However, sometimes the possibility of obtaining the metabolites is limited due to the reduction of wild-growing plants. That is why the plant cell cultures are of great interest as alternative sources of biologically active substances. Besides, during the monitored cultivation, it is possible to obtain substances that are not synthesized by plants in nature. Isolated culture of Ajuga genevensis with high growth activity and ability of regeneration was obtained using MS nutrient medium. The agar-diffusion method showed that aqueous extracts of callus culture revealed high antimicrobial activity towards various gram-positive (Bacillus subtilis A1WT; B. mesentericus WDCM 1873; Staphylococcus aureus WDCM 5233; Staph. citreus WT) and gram-negative (Escherichia coli WKPM M-17; Salmonella typhimurium TA 100) microorganisms. The broth dilution method revealed that the minimal and half maximal inhibitory concentration values against E. coli corresponded to the 70 μg/mL and 140 μg/mL concentration of the extract respectively. According to the photochemiluminescent analysis, callus tissue extracts of leaf and root origin showed higher antioxidant activity than the same quantity of A. genevensis intact plant extract. A. genevensis intact plant and callus culture extracts showed no cytotoxic effect on K-562 suspension cell line of human chronic myeloid leukemia. The GC-MS analysis showed deep differences between the qualitative and quantitative composition of callus culture and intact plant extracts. Hexacosane (11.17%); n-hexadecanoic acid (9.33%); and 2-methoxy-4-vinylphenol (4.28%) were the main components of intact plant extracts. 10-Methylnonadecane (57.0%); methoxyacetic acid, 2-tetradecyl ester (17.75%) and 1-Bromopentadecane (14.55%) were the main components of A. genevensis callus culture extracts. Obtained data indicate that callus culture of A. genevensis can be used as an alternative source of biologically active substances.

Keywords: Ajuga genevensis, antibacterial activity, antioxidant activity, callus cultures

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Authors: Kobus-Cisowska Joanna, Flaczyk Ewa, Gramza-Michalowska Anna, Kmiecik Dominik, Przeor Monika, Marcinkowska Agata

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In recent years, proceed to the attractiveness of typical bakery products. Expanding the education and nutrition knowledge society will develop the production of functional foods, which has a positive impact on human health. Therefore, the aim of the present study was to evaluate the effect of the addition of white mulberry fruit on the content of biologically active compounds in the new designed functional bread premixes designed for selected disease: anemia, diabetes, obesity and cardiovascular disease. For flavonols and phenolic acids content UPLC was conducted, using an NovaPack C18 column and a gradient elution system. It was found that all attempts bread characterized by a high content of biologically active compounds: polyphenols, phenolic acids, and flavonoids. The highest total content of polyphenolic compounds found in the samples of bread for anemia, diabetes and cardiovascular disease both before and after storage. The analyzed sample differed in content of phenolic acids. The highest content of these compounds were found in samples of bread for anemia and diabetes. It was found that the analyzed sample contained phenolic acids that are derivatives of hydroxybenzoic and hydroxycinnamic acid. The new designed bread contained significant amounts of flavonols, of which the dominant was routine.

Keywords: mulberry, antioxidant, polyphenols, phenolic acids, flavonols

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Authors: Shen Jian, Hu Jie, Zhu Guo Niu, Peng Ying Hong

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There are two issues exited in the traditional visual prosthesis: lacking systematic method and the low level of humanization. To tackcle those obstacles, a visual prosthesis design method based on biologically inspired design is proposed. Firstly, a constrained FBS knowledge cell model is applied to construct the functional model of visual prosthesis in biological field. Then the clustering results of engineering domain are ob-tained with the use of the cross-domain knowledge cell clustering algorithm. Finally, a prototype system is designed to support the bio-logically inspired design where the conflict is digested by TRIZ and other tools, and the validity of the method is verified by the solution scheme

Keywords: knowledge-based engineering, visual prosthesis, biologically inspired design, biomedical engineering

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Authors: Ilze Beitane, Evita Straumite

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The aim of the research was to evaluate the influence of flakes from biologically activated hull-less barley grain and malt extract on quality of yoghurt during its storage. The results showed that the concentration of added malt extract and storage time influenced the changes of pH and lactic acid in yoghurt samples. Sensory properties-aroma, taste, consistency and appearance-of yoghurt enriched with flakes from biologically activated hull-less barley grain and malt extract changed significantly (p<0.05) during storage. Yoghurt with increased proportion of malt extract had sweeter taste and more flowing consistency. Sensory properties (taste, aroma, consistency, and appearance) of yoghurt samples enriched with 5% flakes from biologically activated hull-less barley grain (YFBG 5%) and 5% flakes from biologically activated hull-less barley grain and 2% malt extract (YFBG 5% ME 2%) did not change significantly during one week of storage.

Keywords: Barley flakes, malt extract, yoghurt, sensory analysis

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Authors: Austin Jiang, Richard M. Salmon, Nicholas W. Morrell, Wei Li

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BMP10 is highly expressed in the developing heart and plays essential roles in cardiogenesis. BMP10 deletion in mice results in embryonic lethality due to impaired cardiac development. In adults, BMP10 expression is restricted to the right atrium, though ventricular hypertrophy is accompanied by increased BMP10 expression in a rat hypertension model. However, reports of BMP10 activity in the circulation are inconclusive. In particular it is not known whether in vivo secreted BMP10 is active or whether additional factors are required to achieve its bioactivity. It has been shown that high-affinity binding of the BMP10 prodomain to the mature ligand inhibits BMP10 signaling activity in C2C12 cells, and it was proposed that prodomain-bound BMP10 (pBMP10) complex is latent. In this study, we demonstrated that the BMP10 prodomain did not inhibit BMP10 signaling activity in multiple endothelial cells, and that recombinant human pBMP10 complex, expressed in mammalian cells and purified under native conditions, was fully active. In addition, both BMP10 in human plasma and BMP10 secreted from the mouse right atrium were fully active. Finally, we confirmed that active BMP10 secreted from mouse right atrium was in the prodomain-bound form. Our data suggest that circulating BMP10 in adults is fully active and that the reported vascular quiescence function of BMP10 in vivo is due to the direct activity of pBMP10 and does not require an additional activation step. Moreover, being an active ligand, recombinant pBMP10 may have therapeutic potential as an endothelial-selective BMP ligand, in conditions characterized by loss of BMP9/10 signaling.

Keywords: bone morphogenetic protein 10 (BMP10), endothelial cell, signal transduction, transforming growth factor beta (TGF-B)

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Authors: Kalakotla Shanker, G. Krishna Mohan

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Nowadays, nanoparticles are being used in pharmacological studies for their exclusive properties such as small size, more surface area, biocompatibility and enhanced solubility. In view of this, the present study aimed to evaluate the antihyperglycemic potential of biologically synthesized silver nanoparticles (BSSNPs) and Gymnema sylvestre (GS) extract. The SEM and SEM analysis divulges that the BSSNPs were spherical in shape. EDAX spectrum exhibits peaks for the presence of silver, carbon, and oxygen atoms in the range of 1.0-3.1 keV. FT-IR reveals the binding properties of active bio-constituents responsible for capping and stabilizing BSSNPs. The results showed increased blood glucose, huge loss in body weight and downturn in plasma insulin. The GS extract (200 mg/kg, 400 mg/kg), BSSNPs (100 mg/kg, 200 mg/kg) and metformin 50 mg/kg were administered to the diabetic rats. BSSNPs at a dose level of 200 mg/kg (b.wt.p.o.) showed significant inhibition of (p<0.001) blood glucose levels as compared with GS extract treated group. The results obtained from study indicate that the BSSNP shows potent anti-diabetic activity.

Keywords: biological silver nanoparticles, G. sylvetre, gymnemic acid, streptozotocin, Wistar rats, antihyperglycemic activity, anti-hyperlipidemic activity

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Authors: Ouahiba Bechiri, Mostefa Abbessi

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In recent year, polyoxometallates are intensely being explored because of their applications as new materiels, structural aesthetics, catalysts, and biologically active compounds. heteropolyanions of general formulae [X2M18O62] n- (X= heteroatom, e.g. P, Si) and (M=W, Mo), known as Dawson-type anions, constitue a special class of polyoxometallate compounds. In this present work, cobalt substituted heteropolyanion Dawson-type [HP2W15Mo3CoO61] were synthesized and characterized by IR spectroscopy, 31 P NMR, cyclic voltammetry.

Keywords: heteropolyanions, nanomaterials, Dawson-type, characterization

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Authors: Mindaugas Liaudanskas, Darius Kviklys, Kristina Zymonė, Raimondas Raudonis, Jonas Viškelis, Norbertas Uselis, Pranas Viškelis, Valdimaras Janulis

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Apples are among the most commonly consumed fruits in the world. Based on data from the year 2014, approximately 84.63 million tons of apples are grown per annum. Apples are widely used in food industry to produce various products and drinks (juice, wine, and cider); they are also used unprocessed. Apples in human diet are an important source of different groups of biological active compounds that can positively contribute to the prevention of various diseases. They are a source of various biologically active substances – especially vitamins, organic acids, micro- and macro-elements, pectins, and phenolic, triterpenic, and other compounds. Triterpenic compounds, which are characterized by versatile biological activity, are the biologically active compounds found in apples that are among the most promising and most significant for human health. A specific analytical procedure including sample preparation and High Performance Liquid Chromatography (HPLC) analysis was developed, optimized, and validated for the detection of triterpenic compounds in the samples of different apples, their peels, and flesh from widespread apple cultivars 'Aldas', 'Auksis', 'Connel Red', 'Ligol', 'Lodel', and 'Rajka' grown in Lithuanian climatic conditions. The conditions for triterpenic compound extraction were optimized: the solvent of the extraction was 100% (v/v) acetone, and the extraction was performed in an ultrasound bath for 10 min. Isocratic elution (the eluents ratio being 88% (solvent A) and 12% (solvent B)) for a rapid separation of triterpenic compounds was performed. The validation of the methodology was performed on the basis of the ICH recommendations. The following characteristics of validation were evaluated: the selectivity of the method (specificity), precision, the detection and quantitation limits of the analytes, and linearity. The obtained parameters values confirm suitability of methodology to perform analysis of triterpenic compounds. Using the optimised and validated HPLC technique, four triterpenic compounds were separated and identified, and their specificity was confirmed. These compounds were corosolic acid, betulinic acid, oleanolic acid, and ursolic acid. Ursolic acid was the dominant compound in all the tested apple samples. The detected amount of betulinic acid was the lowest of all the identified triterpenic compounds. The greatest amounts of triterpenic compounds were detected in whole apple and apple peel samples of the 'Lodel' cultivar, and thus apples and apple extracts of this cultivar are potentially valuable for use in medical practice, for the prevention of various diseases, for adjunct therapy, for the isolation of individual compounds with a specific biological effect, and for the development and production of dietary supplements and functional food enriched in biologically active compounds. Acknowledgements. This work was supported by a grant from the Research Council of Lithuania, project No. MIP-17-8.

Keywords: apples, HPLC, triterpenic compounds, validation

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Authors: Tatjana Rakcejeva, Jelena Zagorska, Elina Zvezdina

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The aim of the current research was to investigate the gassy ozone effect on quality parameters of flaxes made form whole biologically activated wheat grains. The research was accomplished on in year 2012 harvested wheat grains variety ′Zentos′. Grains were washed, wetted; grain biological activation was performed in the climatic chamber up to 24 hours. After biological activation grains was compressed; than flaxes was dried in convective drier till constant moisture content 9±1%. For grain treatment gassy ozone concentration as 0.0002% and treatment time – 6 min was used. In the processed flaxes the content of A and G tocopherol decrease by 23% and by 9%; content of B2 and B6 vitamins – by 11% and by 10%; elaidic acid – by 46%, oleic acid – by 29%; arginine (by 80%), glutamine (by 74%), asparagine and serine (by 68%), valine (by 62%), cysteine (by 54%) and tyrosine (by 47%).

Keywords: gassy ozone, flaxes, biologically activated grains, quality parameters, treatment

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Authors: Galina N. Parshina, Olga N. Shemshura, Ulzhan S. Mukiyanova, Gulnur M. Beisetbayeva

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From a medical point of view some species from the family Lamiaceae Lindl. attract the attention of scientists. Many plant species from this family are used in science and medicine. Some researchers believe that the medicinal properties of these plants are caused by the action on the organism of the individual components (camphor, menthol, thymol, eugenol, phenols, flavonoids, alcohols, and their derivatives) or the entire complex of essential oils. Biologically active substances (BAS), isolated from these medicinal plants can be an effective supplement in the complex treatment of infectious diseases. The substances of the phenolic group such as flavonoids and phenolic acids; and also alkaloids included in the component composition of the plants from the family Lamiaceae Lindl. present the scientific and practical interest for future investigations of their biological activity and development of medicinal products. The research objects are the species from the family Lamiaceae Lindl., cultivated in the North-Kazakhstan region. In this abstract, we present the results of the investigation of polyphenolic complex (flavonoids and phenolic acids) and alkaloids in aqueous and ethanol extracts. Investigation of the qualitative composition of flavonoids in the aqueous extracts showed that the species Monarda Diana contains flavone, Dracocephalum moldavica contains rutin, Ocimum basilicum (purple form) contains both ruin and quercetin. Biochemical analysis revealed that the ethanol extract of Monarda Diana has phenolic acids, similar to protocatechuic and benzoic acids by their chromatographic characteristics. But the aqueous extract contains four phenolic acids, one of which is an analogue of gentisic acid; and the other three are not identified yet. The phenolic acids such as benzoic and gentisic acids identified in ethanol extracts of species Ocimum basilicum (purple form) and Satureja hortensis, correspondingly. But the same phenolic acids did not appear in aqueous extracts. The phenolic acids were not determined neither in the ethanol or aqueous extracts of species Dracocephalum moldavica. The biochemical analysis did not reveal the content of alkaloids in aqueous extracts of investigated plants. However, the alkaloids in the amount of 5-13 components were identified in the ethanolic extracts of plants by the qualitative reactions. The results of analysis with reagent of Dragendorff showed that next amounts of alkaloids were identified in extracts of Monarda Diana (6-7), Satureja hortensis (6), Ocimum basilicum (7-9) and Dracocephalum moldavica (5-6). The reactions with reagent of Van-Urca showed that next amounts of alkaloids were identified in extracts of Monarda Diana (9-12), Satureja hortensis (9-10), two alkaloids of them with Rf6=0,39 and Rf6=0,31 similar to roquefortine), Ocimum basilicum (11) and Dracocephalum moldavica (13, two of them with Rf5=0,34 and Rf5=0,33 by their chromatographic characteristics similar to epikostaklavin).

Keywords: biologically active substances, Lamiaceae, component composition, medicinal plant

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Authors: Sunil Kumar, Sandip Dhole, Deepak Salunke, Chung-ming Sun

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Heterocycles bearing nitrogen, oxygen, and selenium are present in innumerable biologically active compounds. For instance, coumarin containing dicoumarol acts as naturally occurring anticoagulant. 2-Acylamido selenazole works as Store-Operated Calcium (SOC) channel regulator. Therefore, due to biologically significance of selenazole and coumarin and our quest to develop efficient methodologies for the synthesis of complex heterocycles, the trisubstituted angular isocoumarinoselenazole synthesis was proposed and achieved by starting from nitrobenzoic acid derivative, available commercially. Synthetic procedure involves three steps: i) the construction of 2-aminobenzoselenazoles, ii) their regioselective N-alkylation at position-2 and iii) alkyne insertion via Ru catalyzed C-H activation. Transition metal free synthesis of benzoselenazoles was successfully brought about by the addition/elimination reaction via intramolecular C-Se bond formation. In the next step, N-alkylation of selenazole furnished two regioisomers. Both the isomers exhibited different reactivity towards [4+2] alkyne annulation reaction. The fusion of α-pyrone ring on the benzo[1,3-d]selenazole skeleton was achieved via Ru(II)-catalyzed C-H activation and alkyne insertion. As evident from mechanism, the selenazole 'N' plays an important role for the experiential selectivity.

Keywords: alkylation, alkyne insertion, coumarin, selenazole

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Authors: Valiollah Babaeipour, Mahdi Rahaie

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food supplements are rich in specific nutrients and bioactive compounds that eliminate free radicals and improve cellular metabolism. The major bioactive compounds are found in bran and cereal sprouts. Secondary metabolites of these microorganisms have antioxidant properties that can be used alone or in combination with chemotherapy and radiation therapy to treat cancer. Biologically active compounds such as benzoquinone derivatives extracted from fermented wheat germ extract (FWGE) have several positive effects on the overall state of human health and strengthen the immune system. The present work describes the discontinuous fermentation of raw wheat germ for FWGE production through the simultaneous culture process using the probiotic strains of Saccharomyces cerevisiae, Lactobacillus plantarum, and the possibility of using solid waste. To increase production efficiency, first to select important factors in the optimization of each fermentation process, using a factorial statistical scheme of stirring fraction (120 to 200 rpm), dilution of solids to solvent (1 to 8-12), fermentation time (16 to 24 hours) and strain to wheat germ ratio (20% to 50%) were studied and then simultaneous culture was performed to increase the yields of 2 and 6 dimethoxybenzoquinone (2,6-DMBQ). Since 2 and 6 dimethoxy benzoquinone were fermented as the main biologically active compound in wheat germ extract, UV-Vis analysis was performed to confirm the presence of 2 and 6 dimethoxy benzoquinone in the final product. In addition, 2,6-DMBQ of some products was isolated in a non-polar C-18 column and quantified using high performance liquid chromatography (HPLC). Based on our findings, it can be concluded that the increase of 2 and 6 dimethoxybenzoquinone in the simultaneous culture of Saccharomyces cerevisiae - Lactobacillus plantarum compared to pure culture of Saccharomyces cerevisiae (from 1.89 mg / g) to 28.9% (2.66 mg / g) Increased.

Keywords: wheat germ, FWGE, saccharomyces cerevisiae, lactobacillus plantarum, co-culture, 2, 6-DMBQ

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Authors: Jihan Albayati, Kim Abdullah

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This poster focuses on the significance of active learning strategies and their usage in the ESL classroom. Active learning is a big shift from traditional lecturing to active student engagement which can enhance and enrich student learning; therefore, engaging students is the core of this approach. Students learn more when they participate in the process of learning such as discussions, debates, analysis, synthesis, or any form of activity that requires student involvement. In order to achieve active learning, teachers can use different instructional strategies that are conducive to learning and the selection of these strategies depends on student learning outcomes. Active learning techniques must be carefully designed and integrated into the classroom to increase critical thinking and student participation. This poster provides a concise definition of active learning and its importance, instructional strategies, active learning techniques and their impact on student engagement. Also, it demonstrates the differences between passive and active learners.

Keywords: active learning, learner engagement, student-centered, teaching strategies

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Authors: Anna Trusek-Holownia, Andrzej Noworyta

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Using an enzyme of known specificity the hydrolysis of protein was carried out in a controlled manner. The aim was to obtain oligopeptides being the so-called active peptides or their direct precursors. An original way of expression of the protein hydrolysis kinetics was introduced. Peptide bonds contained in the protein were recognized as a diverse-quality substrate for hydrolysis by the applied protease. This assumption was positively verified taking as an example the hydrolysis of albumin by thermolysin. Peptide linkages for this system should be divided into at least four groups. One of them is a group of bonds non-hydrolyzable by this enzyme. These that are broken are hydrolyzed at a rate that differs even by tens of thousands of times. Designated kinetic constants were k'F = 10991.4 L/g.h, k'M = 14.83L/g.h, k'S about 10-1 L/g.h for fast, medium and slow bonds, respectively. Moreover, a procedure for unfolding of the protein, conducive to the improved susceptibility to enzymatic hydrolysis (approximately three-fold increase in the rate) was proposed.

Keywords: peptide bond hydrolysis, kinetics, enzyme specificity, biologically active peptides

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Authors: Hummera Rafique, Aamer Saeed

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

Keywords: ethyl 4-[2-benzamido-4-methylthiazol-3(2H)-yl)]benzoates, ethyl 4-(3-benzoylthioureido) benzoates, antibacterial activity

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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: Chandra Sekhar Singh, P. Chakrapani, B. Arun Jyothi, A. Roja Rani

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The green synthesis of metallic nanoparticles (NPs) involves biocompatible ingredients under physiological conditions of temperature and pressure. Moreover, the biologically active molecules involved in the green synthesis of NPs act as functionalizing ligands, making these NPs more suitable for biomedical applications. Among the most important bioreductants are plant extracts, which are relatively easy to handle, readily available, low cost, and have been well explored for the green synthesis of other nanomaterials. Various types of metallic NPs have already been synthesized using plant extracts. They have wide applicability in various areas such as electronics, catalysis, chemistry, energy, and medicine. Metallic nanoparticles are traditionally synthesized by wet chemical techniques, where the chemicals used are quite often toxic and flammable. In our study, we were described a cost effective and environment friendly technique for green synthesis of silver nanoparticles from 1mM AgNO3 solution through the aqueous extract of Erythrina indica as reducing as well as capping agent. Nanoparticles were characterized using UV–Vis absorption spectroscopy, FTIR, XRD, X-ray diffraction, SEM and TEM analysis showed the average particle size of 30 nm as well as revealed their spherical structure. Further these biologically synthesized nanoparticles were found to be highly toxic against different human pathogens viz. two Gram positive namely Klebsiella pneumonia and Bacillus subtilis bacteria and two were Gram negative bacteria namely Staphylococcus aureus and Escherichia coli (E. coli). This is for the first time reporting that Erythrina indica plant extract was used for the synthesis of nanoparticles.

Keywords: silver nanoparticles, green synthesis, antibacterial activity, FTIR, TEM, SEM

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Authors: Rukshani Wickrama-Arachchi, Tanner Metz, James M. Takacs

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Amines bearing γ-stereocenters are important structural motifs found in many biologically active compounds. Regioselective Rh-catalyzed asymmetric hydroboration of acyclic allylamines is used to synthesize amines bearing chiral β- and γ-boronic esters yields up to 70% with 98:2 enantioselectivity. The major enantiomeric outcome can be independent of starting alkene geometry, revealing that cis/trans-isomerization of alkene can occur before hydroboration. Stereospecific transformations of the newly generated C-B bond illustrates the utility of these chiral synthons.

Keywords: allylamines, borylated amines, chiral amines, hydroboration, rhodium-catalysis

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Authors: Sabina-Adriana Floria, Marius Gavrilescu, Florin Leon, Silvia Curteanu, Costel Anton

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Neuroevolution is a subfield of artificial intelligence used to solve various problems in different application areas. Specifically, neuroevolution is a technique that applies biologically inspired methods to generate neural network architectures and optimize their parameters automatically. In this paper, we use different biologically inspired optimization algorithms in an ensemble strategy with the aim of training multilayer perceptron neural networks, resulting in regression models used to simulate the industrial chemical process of obtaining bricks from silicone-based materials. Installations in the raw ceramics industry, i.e., bricks, are characterized by significant energy consumption and large quantities of emissions. In addition, the initial conditions that were taken into account during the design and commissioning of the installation can change over time, which leads to the need to add new mixes to adjust the operating conditions for the desired purpose, e.g., material properties and energy saving. The present approach follows the study by simulation of a process of obtaining bricks from silicone-based materials, i.e., the modeling and optimization of the process. Optimization aims to determine the working conditions that minimize the emissions represented by nitrogen monoxide. We first use a search procedure to find the best values for the parameters of various biologically inspired optimization algorithms. Then, we propose an adaptive ensemble strategy that uses only a subset of the best algorithms identified in the search stage. The adaptive ensemble strategy combines the results of selected algorithms and automatically assigns more processing capacity to the more efficient algorithms. Their efficiency may also vary at different stages of the optimization process. In a given ensemble iteration, the most efficient algorithms aim to maintain good convergence, while the less efficient algorithms can improve population diversity. The proposed adaptive ensemble strategy outperforms the individual optimizers and the non-adaptive ensemble strategy in convergence speed, and the obtained results provide lower error values.

Keywords: optimization, biologically inspired algorithm, neuroevolution, ensembles, bricks, emission minimization

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Authors: Desta Gebretekle Shiferaw, Balakrishna Kalluraya

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Oxadiazoles and their derivatives with thioether functionalities represent a new and exciting class of physiologically active heterocyclic compounds. Several molecules with these moieties play a vital role in pharmaceuticals because of their diverse biological activities. This paper describes a new class of 1,3,4- oxadiazole-2-thioethers with acetophenone, coumarin, and N-phenyl acetamide residues (S-alkylation), with the hope that the addition of various biologically active molecules will have a synergistic effect on anticancer activity. The structure of the synthesized title compounds was determined by the combined methods of IR, proton-NMR, carbon-13-NMR, and mass spectrometry. Further, all the newly prepared molecules were assessed against their antioxidant activity. Furthermore, four compounds were assessed for their molecular docking interactions and cytotoxicity activity. The synthesized derivatives have shown moderate antioxidant activity compared to the standard BHA. The IC50 of the tilted molecules (11b, 11c, 13b, and 14b) observed for in vitro anti-cancer activities were 11.20, 15.73, 59.61, and 27.66 g/ml at 72-hour treatment time against the A549 cell lines, respectively. The tested compounds' biological evaluation showed that 11b is the most effective molecule in the series.

Keywords: antioxidant activity, cytotoxicity activity, molecular docking, 1, 3, 4-Oxadiazole-2 thioether derivatives

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Authors: Munir Ashraf, Shagufta Riaz

Abstract:

Personal protective equipment (PPE) and bioactive textiles are highly important for the health care of front line hospital workers, patients, and the general population to be safe from highly infectious diseases. This was even more critical in the wake of COVID-19 outbreak. Most of the medical textiles are inactive against various viruses and bacteria, hence there is a need to wash them frequently to avoid the spread of microorganisms. According to survey conducted by the world health organization, more than 500 million people get infected from hospitals, and more than 13 million died due to these hospitals’ acquired deadly diseases. The market available PPE are though effective against the penetration of pathogens and to kill bacteria but, they are not breathable and active against different viruses. Therefore, there was a great need to develop textiles that are not only effective against bacteria, fungi, and viruses but also are comfortable to the medical personnel and patients. In the present study, waterproof breathable, and biologically active textiles were developed using antiviral and antibacterial nanomaterials. These nanomaterials like TiO₂, ZnO, Cu, and Ag were immobilized at the surface of cotton fabric by using different silane coupling agents and electroless deposition that they retained their functionality even after 30 industrial laundering cycles. Afterwards, the treated fabrics were coated with a waterproof breathable film to prevent the permeation of liquid droplets, any particle or microorganisms greater than 80 nm. The developed cotton fabric was highly active against bacteria and viruses. The good durability of nanomaterials at the cotton surface after several industrial washing cycles makes this fabric an ideal candidate for bioactive textiles used in the medical field.

Keywords: antibacterial, antiviral, cotton, durable

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Authors: Amarjyoti Das Mahapatra, Umesh Kumar, Bhaskar Datta

Abstract:

A pseudo peptide can mimic the biological or structural properties of natural peptides. They have become an increasing attention in medicinal chemistry because of their interesting advantages like more bioavailability and less biodegradation than compare to the physiologically active native peptides which increase their therapeutic applications. Many biologically active compounds contain urea as functional groups, and they have improved pharmacokinetic properties because of their bioavailability and metabolic stability. Recently we have reported a single-step synthesis of sulfonyl urea and sulfonyltriuret from sulfonyl chloride and sodium cyanate. But the yield of sulfonyltriuret was less around 40-60% because of the formation of other products like sulfonamide and sulfonylureas. In the present work, we mainly focused on the selective synthesis of sulfonyltriuret using tetrabutylammonium cyanate and sulfonyl chloride. More precisely, we are interested in the controlled synthesis of oligomeric urea mainly sulfonyltriuret as a new class of pseudo peptide and their application as protease modulators. The distinctive architecture of these molecules in the form of their pseudo-peptide backbone offers promise as a potential pharmacophore. The synthesized molecules have been screened on trypsin enzyme, and we observed that these molecules are the efficient modulator of trypsin enzyme.

Keywords: pseudo peptide, pharmacophore, sulfonyltriuret, trypsin

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Authors: V. Barbakadze, L. Gogilashvili, L. Amiranashvili, M. Merlani, K. Mulkijanyan

Abstract:

The high-molecular water-soluble preparations from several species of two genera (Symphytum and Anchusa) of Boraginaceae family Symphytum asperum, S. caucasicum, S.officinale and Anchusa italica were isolated. According to IR, 13C and 1H NMR, APT, 1D NOE, 2D heteronuclear 1H/13C HSQC and 2D DOSY experiments, the main chemical constit¬uent of these preparations was found to be caffeic acid-derived polyether, namely poly[3-(3,4-dihydroxyphenyl)glyceric acid] (PDPGA) or poly[oxy-1-carboxy-2-(3,4-dihydroxyphenyl)ethylene]. Most carboxylic groups of this caffeic acid-derived polymer of A. italica are methylated.

Keywords: Anchusa, poly[3-(3, 4-dihydroxyphenyl)glyceric acid], poly[oxy-1-carboxy-2-(3, 4-dihydroxyphenyl)ethylene], Symphytum

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Authors: Beata Wentura-Dudek

Abstract:

In Sweden the needs of the labor market are regularly monitored. Test results and forecasts translate directly into the education system in this country, which is largely a state system. Sweden is one of the first countries in Europe that has used active labor market policies. It is realized that there is an active unemployment which includes a wide range of activities that can be divided into three groups: Active forms of influencing the creation of new jobs, active forms that affect the labor supply and active forms for people with disabilities. Most of the funding is allocated there for subsidized employment and training. Research conducted in Sweden shows that active forms of counteracting unemployment focused on the long-term unemployed can significantly raise the level of employment in this group.

Keywords: Sweden, research conducted in Sweden, labour market, labour market policies, unemployment, active forms of influencing the creation of new jobs, active forms of counteracting unemployment, employment, subsidized employment education

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Authors: Lamzira Ebralidze, Aleksandre Tsertsvadze, Dali Berashvili, Aliosha Bakuridze

Abstract:

Nowadays, there is an increasing demand for biologically active substances from vegetable, animal, and mineral resources. In terms of the use of natural compounds, pharmaceutical, cosmetic, and nutrition industry has big interest. The biggest drawback of conventional extraction methods is the need to use a large volume of organic extragents. The removal of the organic solvent is a multi-stage process. And their absolute removal cannot be achieved, and they still appear in the final product as impurities. A large amount of waste containing organic solvent damages not only human health but also has the harmful effects of the environment. Accordingly, researchers are focused on improving the extraction methods, which aims to minimize the use of organic solvents and energy sources, using alternate solvents and renewable raw materials. In this context, green extraction principles were formed. Green Extraction is a need of today’s environment. Green Extraction is the concept, and it totally corresponds to the challenges of the 21st century. The extraction of biologically active compounds based on green extraction principles is vital from the view of preservation and maintaining biodiversity. Novel technologies of green extraction are known, such as "cold methods" because during the extraction process, the temperature is relatively lower, and it doesn’t have a negative impact on the stability of plant compounds. Novel technologies provide great opportunities to reduce or replace the use of organic toxic solvents, the efficiency of the process, enhance excretion yield, and improve the quality of the final product. The objective of the research is the development of green technologies of flavonoids containing preparations. Methodology: At the first stage of the research, flavonoids containing preparations (Tincture Herba Leonuri, flamine, rutine) were prepared based on conventional extraction methods: maceration, bismaceration, percolation, repercolation. At the same time, the same preparations were prepared based on green technologies, microwave-assisted, UV extraction methods. Product quality characteristics were evaluated by pharmacopeia methods. At the next stage of the research technological - economic characteristics and cost efficiency of products prepared based on conventional and novel technologies were determined. For the extraction of flavonoids, water is used as extragent. Surface-active substances are used as co-solvent in order to reduce surface tension, which significantly increases the solubility of polyphenols in water. Different concentrations of water-glycerol mixture, cyclodextrin, ionic solvent were used for the extraction process. In vitro antioxidant activity will be studied by the spectrophotometric method, using DPPH (2,2-diphenyl-1- picrylhydrazyl) as an antioxidant assay. The advantage of green extraction methods is also the possibility of obtaining higher yield in case of low temperature, limitation extraction process of undesirable compounds. That is especially important for the extraction of thermosensitive compounds and maintaining their stability.

Keywords: extraction, green technologies, natural resources, flavonoids

Procedia PDF Downloads 98