WorldWideScience

Sample records for nonnatural bioactive derivatives

  1. Quinazoline derivatives: synthesis and bioactivities

    OpenAIRE

    Wang, Dan; Gao, Feng

    2013-01-01

    Owing to the significant biological activities, quinazoline derivatives have drawn more and more attention in the synthesis and bioactivities research. This review summarizes the recent advances in the synthesis and biological activities investigations of quinazoline derivatives. According to the main method the authors adopted in their research design, those synthetic methods were divided into five main classifications, including Aza-reaction, Microwave-assisted reaction, Metal-mediated reac...

  2. Food-derived bioactive peptides on inflammation and oxidative stress.

    Science.gov (United States)

    Chakrabarti, Subhadeep; Jahandideh, Forough; Wu, Jianping

    2014-01-01

    Chronic diseases such as atherosclerosis and cancer are now the leading causes of morbidity and mortality worldwide. Inflammatory processes and oxidative stress underlie the pathogenesis of these pathological conditions. Bioactive peptides derived from food proteins have been evaluated for various beneficial effects, including anti-inflammatory and antioxidant properties. In this review, we summarize the roles of various food-derived bioactive peptides in inflammation and oxidative stress and discuss the potential benefits and limitations of using these compounds against the burden of chronic diseases.

  3. De novo Biosynthesis of "Non-Natural" Thaxtomin Phytotoxins.

    Science.gov (United States)

    Winn, Michael; Francis, Daniel; Micklefield, Jason

    2018-03-30

    Thaxtomins are diketopiperazine phytotoxins produced by Streptomyces scabies and other actinobacterial plant pathogens that inhibit cellulose biosynthesis in plants. Due to their potent bioactivity and novel mode of action there has been considerable interest in developing thaxtomins as herbicides for crop protection. To address the need for more stable derivatives, we have developed a new approach for structural diversification of thaxtomins. Genes encoding the thaxtomin NRPS from S. scabies, along with genes encoding a promiscuous tryptophan synthase (TrpS) from Salmonella typhimurium, were assembled in a heterologous host Streptomyces albus. Upon feeding indole derivatives to the engineered S. albus strain, tryptophan intermediates with alternative substituents are biosynthesized and incorporated by the NRPS to deliver a series of thaxtomins with different functionalities in place of the nitro group. The approach described herein, demonstrates how genes from different pathways and different bacterial origins can be combined in a heterologous host to create a de novo biosynthetic pathway to "non-natural" product target compounds. © 2018 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.

  4. Investigation of bioactivity and cell effects of nano-porous sol–gel derived bioactive glass film

    Energy Technology Data Exchange (ETDEWEB)

    Ma, Zhijun, E-mail: mokuu@zju.edu.cn [State Key Laboratory of Luminescent Materials and Devices, South China University of Technology, Guangzhou, 510640 (China); Ji, Huijiao [College of Life Science, Zhejiang University, Hangzhou, 310028 (China); Hu, Xiaomeng [School of Materials Science and Engineering, South China University of Technology, Guangzhou, 510640 (China); Teng, Yu [State Key Laboratory of Luminescent Materials and Devices, South China University of Technology, Guangzhou, 510640 (China); Zhao, Guiyun; Mo, Lijuan; Zhao, Xiaoli [College of Life Science, Zhejiang University, Hangzhou, 310028 (China); Chen, Weibo [School of Materials Science and Engineering, South China University of Technology, Guangzhou, 510640 (China); Qiu, Jianrong, E-mail: qjr@scut.edu.cn [State Key Laboratory of Luminescent Materials and Devices, South China University of Technology, Guangzhou, 510640 (China); Zhang, Ming, E-mail: zhangming201201@126.com [College of Life Science, Zhejiang University, Hangzhou, 310028 (China)

    2013-11-01

    In orthopedic surgery, bioactive glass film coating is extensively studied to improve the synthetic performance of orthopedic implants. A lot of investigations have confirmed that nano-porous structure in bioactive glasses can remarkably improve their bioactivity. Nevertheless, researches on preparation of nano-porous bioactive glasses in the form of film coating and their cell response activities are scarce. Herein, we report the preparation of nano-porous bioactive glass film on commercial glass slide based on a sol–gel technique, together with the evaluation of its in vitro bioactivity through immersion in simulated body fluid and monitoring the precipitation of apatite-like layer. Cell responses of the samples, including attachment, proliferation and osteogenic differentiation, were also investigated using BMSCS (bone marrow derived mesenchymal stem cells) as a model. The results presented here provide some basic information on structural influence of bioactive glass film on the improvement of bioactivity and cellular effects.

  5. Investigation of bioactivity and cell effects of nano-porous sol-gel derived bioactive glass film

    Science.gov (United States)

    Ma, Zhijun; Ji, Huijiao; Hu, Xiaomeng; Teng, Yu; Zhao, Guiyun; Mo, Lijuan; Zhao, Xiaoli; Chen, Weibo; Qiu, Jianrong; Zhang, Ming

    2013-11-01

    In orthopedic surgery, bioactive glass film coating is extensively studied to improve the synthetic performance of orthopedic implants. A lot of investigations have confirmed that nano-porous structure in bioactive glasses can remarkably improve their bioactivity. Nevertheless, researches on preparation of nano-porous bioactive glasses in the form of film coating and their cell response activities are scarce. Herein, we report the preparation of nano-porous bioactive glass film on commercial glass slide based on a sol-gel technique, together with the evaluation of its in vitro bioactivity through immersion in simulated body fluid and monitoring the precipitation of apatite-like layer. Cell responses of the samples, including attachment, proliferation and osteogenic differentiation, were also investigated using BMSCS (bone marrow derived mesenchymal stem cells) as a model. The results presented here provide some basic information on structural influence of bioactive glass film on the improvement of bioactivity and cellular effects.

  6. Marine-Derived Bioactive Peptides with Pharmacological Activities- A Review

    Directory of Open Access Journals (Sweden)

    Sana Rabiei

    2017-10-01

    Full Text Available Some nutritional factors are related to chronic disease. In response to increased concern regarding nutrition and health, the functional and nutraceuticals food markets have been developed. During food digestion, proteins are hydrolyzed and a wide range of peptides are formed. Some of these peptides have special structures which permit them to confer particular biological functions. Marine animals which involve more than half of the world biological varieties are a wide source of bioactive proteins and peptides. Marine derived peptides show various physiologic functions such as anti-oxidant, antimicrobial, anti-cancer, Angiotensin1-Converting Enzyme (ACE glucosidase and a-amylase inhibitory effects in vitro. Before application of marine bioactive peptides as nutraceuticals or functional food ingredients, their efficacy should be approved through pre-clinical animal and then clinical studies. The aim of this study was to review the studies conducted on the pharmacological effect of marine bioactive peptides in animal models and humans.

  7. Bioactive benzopyrone derivatives from new recombinant fusant of marine Streptomyces.

    Science.gov (United States)

    El-Gendy, Mervat M A; Shaaban, M; El-Bondkly, A M; Shaaban, K A

    2008-07-01

    In our searching program for bioactive secondary metabolites from marine Streptomycetes, three microbial benzopyrone derivatives (1-3), 7-methylcoumarin (1) and two flavonoides, rhamnazin (2) and cirsimaritin (3), were obtained during the working up of the ethyl acetate fraction of a marine Streptomyces fusant obtained from protoplast fusion between Streptomyces strains Merv 1996 and Merv 7409. The structures of the three compounds (1-3) were established by nuclear magnetic resonance, mass, UV spectra, and by comparison with literature data. Marine Streptomyces strains were identified based on their phenotypic and chemotypic characteristics as two different bioactive strains of the genus Streptomyces. We described here the fermentation, isolation, as well as the biological activity of these bioactive compounds. The isolated compounds (1-3) are reported here as microbial products for the first time.

  8. Structural and Energetic Impact of Non-Natural 7-Deaza-8-Azaadenine and its 7-Substituted Derivatives on H-Bonding Potential with Uracil in RNA Molecules

    KAUST Repository

    Chawla, Mohit; Credendino, Raffaele; Oliva, Romina; Cavallo, Luigi

    2015-01-01

    Non-natural (synthetic) nucleobases, including 7-ethynyl- and 7-triazolyl-8-aza-7-deazaadenosine, have been introduced in RNA molecules for targeted applications, and have been characterized experimentally. However, no theoretical characterization of the impact of these modifications on the structure and energetics of the corresponding H-bonded base pair is available. To fill this gap, we performed quantum mechanics calculations, starting with the analysis of the impact of the 8-aza-7-deaza modification of the adenosine skeleton, and we moved then to analyze the impact of the specific substituents on the modified 8-aza-7-deazaadenosine. Our analysis indicates that, despite of these severe structural modifications, the H-bonding properties of the modified base pair gratifyingly replicate those of the unmodified base pair. Similar behavior is predicted when the same skeleton modifications are applied to guanosine when paired to cytosine. To stress further the H-bonding pairing in the modified adenosine-uracil base pair, we explored the impact of strong electron donor and electron withdrawing substituents on the C7 position. Also in this case we found minimal impact on the base pair geometry and energy, confirming the validity of this modification strategy to functionalize RNAs without perturbing its stability and biological functionality.

  9. Structural and Energetic Impact of Non-Natural 7-Deaza-8-Azaadenine and its 7-Substituted Derivatives on H-Bonding Potential with Uracil in RNA Molecules

    KAUST Repository

    Chawla, Mohit

    2015-09-21

    Non-natural (synthetic) nucleobases, including 7-ethynyl- and 7-triazolyl-8-aza-7-deazaadenosine, have been introduced in RNA molecules for targeted applications, and have been characterized experimentally. However, no theoretical characterization of the impact of these modifications on the structure and energetics of the corresponding H-bonded base pair is available. To fill this gap, we performed quantum mechanics calculations, starting with the analysis of the impact of the 8-aza-7-deaza modification of the adenosine skeleton, and we moved then to analyze the impact of the specific substituents on the modified 8-aza-7-deazaadenosine. Our analysis indicates that, despite of these severe structural modifications, the H-bonding properties of the modified base pair gratifyingly replicate those of the unmodified base pair. Similar behavior is predicted when the same skeleton modifications are applied to guanosine when paired to cytosine. To stress further the H-bonding pairing in the modified adenosine-uracil base pair, we explored the impact of strong electron donor and electron withdrawing substituents on the C7 position. Also in this case we found minimal impact on the base pair geometry and energy, confirming the validity of this modification strategy to functionalize RNAs without perturbing its stability and biological functionality.

  10. Food Derived Bioactive Peptides and Intestinal Barrier Function

    Directory of Open Access Journals (Sweden)

    Olga Martínez-Augustin

    2014-12-01

    Full Text Available A wide range of food-derived bioactive peptides have been shown to exert health-promoting actions and are therefore considered functional foods or nutraceuticals. Some of these actions are related to the maintenance, reinforcement or repairment of the intestinal barrier function (IBF whose role is to selectively allow the absorption of water, nutrients and ions while preventing the influx of microorganisms from the intestinal lumen. Alterations in the IBF have been related to many disorders, such as inflammatory bowel disease or metabolic syndrome. Components of IBF are the intestinal epithelium, the mucus layer, secretory immunoglobulin A and cells of the innate and adaptive immune systems. Here we review the effects of food derived bioactive peptides on these IBF components. In vitro and in vivo effects, both in healthy and disease states, have been reviewed. Although limited, the available information indicates a potential for food-derived peptides to modify IBF and to contribute to disease treatment, but further research is needed to better isolate responsible peptides, and to help define their mode of action.

  11. Proficient synthesis of bioactive annulated pyrimidine derivatives: A review

    Directory of Open Access Journals (Sweden)

    Ajmal R. Bhat

    2017-11-01

    Full Text Available Syntheses of bioactive annulated pyrimidine derivatives are the most significant tasks in N-heterocyclic chemistry because these compounds have proved to be very attractive and useful for the design of new molecular frameworks of potential drugs with varying pharmacological activities. This review paper summarizes the one-pot multicomponent synthesis of annulated nitrogen- and oxygen-containing heterocycles, such as pyrano[2,3-d]pyrimidines, pyrido[2,3-d]pyrimidines and pyrido[2,3-d;5-6-d]dipyrimidines. The synthetic procedure is based on the chemistry of the domino Knoevenagel-Michael addition mechanism. Keywords: Pyrano[2,3-d]pyrimidines, Pyrido[2,3-d]pyrimidines, Pyrido[2,3-d;5-6-d]dipyrimidines, Barbituric acid/Thio-barbituric acid, Aromatic aldehydes, 6-aminouracil

  12. Sol-gel derived porous bioactive nanocomposites: Synthesis and in vitro bioactivity

    Science.gov (United States)

    Shankhwar, Nisha; Kothiyal, G. P.; Srinivasan, A.

    2013-06-01

    Porous bioactive composites consisting of SiO2-CaO-Na2O-P2O5 bioactive glass-ceramic and synthetic water soluble polymer Polyvinylpyrrolidone [PVP (C6H9NO)n, MW˜40000 g/mol] have been synthesized by sol-gel route. As-prepared polymeric composites were characterized by X-ray diffraction (XRD) technique. Two major bone mineral phases, viz., hydroxyapatite [Ca10(PO4)6(OH)2] and wollastonite [calcium silicate (CaSiO3)] have been identified in the XRD patterns of the composites. Presence of these bone minerals indicates the bioactive nature of the composites. In vitro bioactivity tests confirm bioactivity in the porous composites. The flexibility offered by these bioactive polymer composites is advantageous for its application as implant material.

  13. Characterization of the bioactive and mechanical behavior of dental ceramic/sol-gel derived bioactive glass mixtures.

    Science.gov (United States)

    Abbasi, Zahra; Bahrololoum, Mohammad E; Bagheri, Rafat; Shariat, Mohammad H

    2016-02-01

    Dental ceramics can be modified by bioactive glasses in order to develop apatite layer on their surface. One of the benefits of such modification is to prolong the lifetime of the fixed dental prosthesis by preventing the formation of secondary caries. Dental ceramic/sol-gel derived bioactive glass mixture is one of the options for this modification. In the current study, mixtures of dental ceramic/bioactive glass with different compositions were successfully produced. To evaluate their bioactive behavior, prepared samples were immersed in a simulated body fluid at various time intervals. The prepared and soaked specimens were characterized using Fourier transform infrared spectroscopy, X-ray diffractometry and scanning electron microscopy. Since bioactive glasses have deleterious effects on the mechanical properties of dental ceramics, 3-point bending tests were used to evaluate the flexural strength, flexural strain, tangent modulus of elasticity and Weibull modulus of the specimens in order to find the optimal relationship between mechanical and bioactive properties. Copyright © 2015 Elsevier Ltd. All rights reserved.

  14. Bioactive cembrane derivatives from the Indian Ocean soft coral, Sinularia kavarattiensis.

    Digital Repository Service at National Institute of Oceanography (India)

    Lillsunde, K.-E.; Festa, C.; Adel, H.; DeMarino, S.; Lombardi, V.; Tilvi, S.; Nawrot, D.A.; Zampella, A.; DeSouza, L.; DeAuria, M.V.; Tammela, P.

    Marine organisms and their metabolites represent a unique source of potential pharmaceutical substances. In this study, we examined marine-derived substances for their bioactive properties in a cell-based Chikungunya virus (CHIKV) replicon model...

  15. BioPepDB: an integrated data platform for food-derived bioactive peptides.

    Science.gov (United States)

    Li, Qilin; Zhang, Chao; Chen, Hongjun; Xue, Jitong; Guo, Xiaolei; Liang, Ming; Chen, Ming

    2018-03-12

    Food-derived bioactive peptides play critical roles in regulating most biological processes and have considerable biological, medical and industrial importance. However, a large number of active peptides data, including sequence, function, source, commercial product information, references and other information are poorly integrated. BioPepDB is a searchable database of food-derived bioactive peptides and their related articles, including more than four thousand bioactive peptide entries. Moreover, BioPepDB provides modules of prediction and hydrolysis-simulation for discovering novel peptides. It can serve as a reference database to investigate the function of different bioactive peptides. BioPepDB is available at http://bis.zju.edu.cn/biopepdbr/ . The web page utilises Apache, PHP5 and MySQL to provide the user interface for accessing the database and predict novel peptides. The database itself is operated on a specialised server.

  16. Bioactive Properties of Maillard Reaction Products Generated From Food Protein-derived Peptides.

    Science.gov (United States)

    Arihara, K; Zhou, L; Ohata, M

    Food protein-derived peptides are promising food ingredients for developing functional foods, since various bioactive peptides are released from food proteins. The Maillard reaction, which plays an important role in most processed foods, generates various chemical components during processing. Although changes of amino acids or proteins and reduced sugars by the Maillard reaction have been studied extensively, such changes of peptides by the Maillard reaction are still not resolved enough. Since food protein-derived peptides are widely utilized in many processed foods, it deserves concern and research on the changes of peptides by the Maillard reaction in foods during processing or storage. This chapter initially overviewed food protein-derived bioactive peptides. Then, Maillard reaction products generated from peptides are discussed. We focused particularly on their bioactivities. © 2017 Elsevier Inc. All rights reserved.

  17. Milk derived bioactive peptides and their impact on human health – A review

    Directory of Open Access Journals (Sweden)

    D.P. Mohanty

    2016-09-01

    Full Text Available Milk-derived bioactive peptides have been identified as potential ingredients of health-promoting functional foods. These bioactive peptides are targeted at diet-related chronic diseases especially the non-communicable diseases viz., obesity, cardiovascular diseases and diabetes. Peptides derived from the milk of cow, goat, sheep, buffalo and camel exert multifunctional properties, including anti-microbial, immune modulatory, anti-oxidant, inhibitory effect on enzymes, anti-thrombotic, and antagonistic activities against various toxic agents. Majority of those regulate immunological, gastrointestinal, hormonal and neurological responses, thereby playing a vital role in the prevention of cancer, osteoporosis, hypertension and other disorders as discussed in this review. For the commercial production of such novel bioactive peptides large scale technologies based on membrane separation and ion exchange chromatography methods have been developed. Separation and identification of those peptides and their pharmacodynamic parameters are necessary to transfer their potent functional properties into food applications. The present review summarizes the preliminary classes of bioactive milk-derived peptides along with their physiological functions, general characteristics and potential applications in health-care.

  18. Bioalerts: a python library for the derivation of structural alerts from bioactivity and toxicity data sets.

    Science.gov (United States)

    Cortes-Ciriano, Isidro

    2016-01-01

    Assessing compound toxicity at early stages of the drug discovery process is a crucial task to dismiss drug candidates likely to fail in clinical trials. Screening drug candidates against structural alerts, i.e. chemical fragments associated to a toxicological response prior or after being metabolized (bioactivation), has proved a valuable approach for this task. During the last decades, diverse algorithms have been proposed for the automatic derivation of structural alerts from categorical toxicity data sets. Here, the python library bioalerts is presented, which comprises functionalities for the automatic derivation of structural alerts from categorical (dichotomous), e.g. toxic/non-toxic, and continuous bioactivity data sets, e.g. [Formula: see text] or [Formula: see text] values. The library bioalerts relies on the RDKit implementation of the circular Morgan fingerprint algorithm to compute chemical substructures, which are derived by considering radial atom neighbourhoods of increasing bond radius. In addition to the derivation of structural alerts, bioalerts provides functionalities for the calculation of unhashed (keyed) Morgan fingerprints, which can be used in predictive bioactivity modelling with the advantage of allowing for a chemically meaningful deconvolution of the chemical space. Finally, bioalerts provides functionalities for the easy visualization of the derived structural alerts.

  19. Novel Bioactive Paulomycin Derivatives Produced by Streptomyces albus J1074

    Directory of Open Access Journals (Sweden)

    Jorge Fernández-De la Hoz

    2017-10-01

    Full Text Available Four novel paulomycin derivatives have been isolated from S. albus J1074 grown in MFE culture medium. These compounds are structural analogs of antibiotics 273a2α and 273a2β containing a thiazole moiety, probably originated through an intramolecular Michael addition. The novel, thiazole, moiety-containing paulomycins show a lower antibiotic activity than paulomycins A and B against Gram-positive bacteria. However, two of them show an improved activity against Gram-negative bacteria. In addition, the four novel compounds are more stable in culture than paulomycins A and B. Thus, the presence of an N-acetyl-l-cysteine moiety linked to the carbon atom of the paulic acid isothiocyanate moiety, via a thioester bond, and the subsequent intramolecular cyclization of the paulic acid to generate a thiazole heterocycle confer to paulomycins a higher structural stability that otherwise will conduce to paulomycin degradation and into inactive paulomenols.

  20. Efficient Synthesis and Bioactivity of Novel Triazole Derivatives.

    Science.gov (United States)

    Hu, Boyang; Zhao, Hanqing; Chen, Zili; Xu, Chen; Zhao, Jianzhuang; Zhao, Wenting

    2018-03-21

    Triazole pesticides are organic nitrogen-containing heterocyclic compounds, which contain 1,2,3-triazole ring. In order to develop potential glucosamine-6-phosphate synthase (GlmS) inhibitor fungicides, forty compounds of triazole derivatives were synthesized in an efficient way, thirty nine of them were new compounds. The structures of all the compounds were confirmed by high resolution mass spectrometer (HRMS), ¹H-NMR and 13 C-NMR. The fungicidal activities results based on means of mycelium growth rate method indicated that some of the compounds exhibited good fungicidal activities against P. CapasiciLeonian , Sclerotinia sclerotiorum (Lib.) de Bary, Pyricularia oryzae Cav. and Fusarium oxysporum Schl. F.sp. vasinfectum (Atk.) Snyd. & Hans. at the concentration of 50 µg/mL, especially the inhibitory rates of compounds 1-d and 1-f were over 80%. At the same time, the preliminary studies based on the Elson-Morgan method indicated that the compounds exhibited some inhibitory activity toward glucosamine-6-phosphate synthase (GlmS). These compounds will be further studied as potential antifungal lead compounds. The structure-activity relationships (SAR) were discussed in terms of the effects of the substituents on both the benzene and the sugar ring.

  1. Efficient Synthesis and Bioactivity of Novel Triazole Derivatives

    Directory of Open Access Journals (Sweden)

    Boyang Hu

    2018-03-01

    Full Text Available Triazole pesticides are organic nitrogen-containing heterocyclic compounds, which contain 1,2,3-triazole ring. In order to develop potential glucosamine-6-phosphate synthase (GlmS inhibitor fungicides, forty compounds of triazole derivatives were synthesized in an efficient way, thirty nine of them were new compounds. The structures of all the compounds were confirmed by high resolution mass spectrometer (HRMS, 1H-NMR and 13C-NMR. The fungicidal activities results based on means of mycelium growth rate method indicated that some of the compounds exhibited good fungicidal activities against P. CapasiciLeonian, Sclerotinia sclerotiorum (Lib. de Bary, Pyricularia oryzae Cav. and Fusarium oxysporum Schl. F.sp. vasinfectum (Atk. Snyd. & Hans. at the concentration of 50 µg/mL, especially the inhibitory rates of compounds 1-d and 1-f were over 80%. At the same time, the preliminary studies based on the Elson-Morgan method indicated that the compounds exhibited some inhibitory activity toward glucosamine-6-phosphate synthase (GlmS. These compounds will be further studied as potential antifungal lead compounds. The structure-activity relationships (SAR were discussed in terms of the effects of the substituents on both the benzene and the sugar ring.

  2. Synthesis and Bioactivity of Pyrazole Acyl Thiourea Derivatives

    Directory of Open Access Journals (Sweden)

    Jian Wu

    2012-05-01

    Full Text Available Sixteen novel pyrazole acyl thiourea derivatives 6 were synthesized from monomethylhydrazine (phenylhydrazine and ethyl acetoacetate. The key 5-chloro-3-methyl-1-substituted-1H-pyrazole-4-carbonyl chloride intermediates 4 were first generated in four steps through cyclization, formylation, oxidation and acylation. Thess were then reacted with ammonium thiocyanate in the presence of PEG-400 to afford 5-chloro-3-methyl-1-substituted-1H-pyrazole-4-carbonyl isothiocyanates 5. Subsequent reaction with fluorinated aromatic amines resulted in the formation of the title compounds. The synthesized compound were unequivocally characterized by IR, 1H-NMR, 13C-NMR and elemental analysis and some of the synthesized compounds displayed good antifungal activities against Gibberella zeae, Fusarium oxysporum, Cytospora mandshurica and anti-TMV activity in preliminary antifungal activity tests.

  3. Bioactivity, mechanical properties and drug delivery ability of bioactive glass-ceramic scaffolds coated with a natural-derived polymer.

    Science.gov (United States)

    Araújo, M; Viveiros, R; Philippart, A; Miola, M; Doumett, S; Baldi, G; Perez, J; Boccaccini, A R; Aguiar-Ricardo, A; Verné, E

    2017-08-01

    In this work, hybrid melanin-coated bioactive glass-ceramic multifunctional scaffolds were developed and characterized in terms of mechanical strength, in vitro bioactivity in simulated body fluid (SBF) and ability to load ibuprofen. The coated scaffolds exhibited an accelerated bioactivity in comparison with the uncoated ones, being able of developing hydroxyapatite-like crystals after 7days soaking in simulated body fluid (SBF). Besides its positive influence on the scaffolds bioactivity, the melanin coating was able to enhance their mechanical properties, increasing the initial compressive strength by a factor of >2.5. Furthermore, ibuprofen was successfully loaded on this coating, allowing a controlled drug release of the anti-inflammatory agent. Copyright © 2017 Elsevier B.V. All rights reserved.

  4. The Evaluation and Utilization of Marine-derived Bioactive Compounds with Anti-obesity Effect.

    Science.gov (United States)

    Jin, Qiu; Yu, Huahua; Li, Pengcheng

    2018-01-01

    Obesity is a global epidemic throughout the world. There is thus increasing interest in searching for natural bioactive compounds with anti-obesity effect. A number of marine compounds have been regarded as potential sources of bioactive compounds and are associated with an anti-obesity effect. Marine-derived compounds with anti-obesity effect and their current applications, methods and indicators for the evaluation of anti-obesity activity are summarized in this review. in order to make contributions to the development of marine-derived functional food against obesity. In this review, an overview of marine-derived compounds with anti-obesity effect, including marine polysaccharides, marine lipid, marine peptides, marine carotenoids is intensively made with an emphasis on their efficacy and mechanism of action. Meanwhile, methods and indicators for the evaluation of anti-obesity activity are discussed. We summarize these methods into three categories: in vitro assay (including adsorption experiments and enzyme inhibitory assay), cell line study, animal experiments and clinical experiments. In addition, a brief introduction of the current applications of marine bioactive compounds with anti-obesity activity is discussed. Marine environment is a rich source of both biological and chemical diversity. In the past decades, numerous novel compounds with anti-obesity activity have been obtained from marine organisms, and many of them have been applied to industrial production such as functional foods and pharmaceuticals. Further studies are needed to explore the above-mentioned facts. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

  5. Effect of calcium source on structure and properties of sol-gel derived bioactive glasses.

    Science.gov (United States)

    Yu, Bobo; Turdean-Ionescu, Claudia A; Martin, Richard A; Newport, Robert J; Hanna, John V; Smith, Mark E; Jones, Julian R

    2012-12-18

    The aim was to determine the most effective calcium precursor for synthesis of sol-gel hybrids and for improving homogeneity of sol-gel bioactive glasses. Sol-gel derived bioactive calcium silicate glasses are one of the most promising materials for bone regeneration. Inorganic/organic hybrid materials, which are synthesized by incorporating a polymer into the sol-gel process, have also recently been produced to improve toughness. Calcium nitrate is conventionally used as the calcium source, but it has several disadvantages. Calcium nitrate causes inhomogeneity by forming calcium-rich regions, and it requires high temperature treatment (>400 °C) for calcium to be incorporated into the silicate network. Nitrates are also toxic and need to be burnt off. Calcium nitrate therefore cannot be used in the synthesis of hybrids as the highest temperature used in the process is typically 40-60 °C. Therefore, a different precursor is needed that can incorporate calcium into the silica network and enhance the homogeneity of the glasses at low (room) temperature. In this work, calcium methoxyethoxide (CME) was used to synthesize sol-gel bioactive glasses with a range of final processing temperatures from 60 to 800 °C. Comparison is made between the use of CME and calcium chloride and calcium nitrate. Using advanced probe techniques, the temperature at which Ca is incorporated into the network was identified for 70S30C (70 mol % SiO(2), 30 mol % CaO) for each of the calcium precursors. When CaCl(2) was used, the Ca did not seem to enter the network at any of the temperatures used. In contrast, Ca from CME entered the silica network at room temperature, as confirmed by X-ray diffraction, (29)Si magic angle spinning nuclear magnetic resonance spectroscopy, and dissolution studies. CME should be used in preference to calcium salts for hybrid synthesis and may improve homogeneity of sol-gel glasses.

  6. Chemical characterization & bioactivity of diketopiperazine derivatives from the mangrove derived Pseudonocardia endophytica

    Directory of Open Access Journals (Sweden)

    Usha Kiranmayi Mangamuri

    2016-06-01

    Full Text Available Sediment samples from the mangrove ecosystem of Nizampatnam have been analyzed for actinomycetes as an elite source to screen for the formulation and production of antimicrobial and cytotoxic compounds. The actinomycetes strain VUK-10 has an interesting bioactivity profile and was isolated during our systematic study of mangrove actinomycetes. It was identified as Pseudonocardia endophytica with the aid of polyphasic taxonomy. The ethyl acetate extract of the actinobacterial culture filtrate has been purified by gel-filtration and silica gel column chromatographic purifications led to the isolation of two diketopiperazine compounds, (3S,8aS-3-isobutylhexahydropyrrolo[1,2-a]pyrazine-1,4-dione (1 and (3R,8aS-3-isobutylhexahydropyrrolo[1,2-a]pyrazine-1,4-dione (2. The compounds listed, alluring cytotoxic activity against MDA-MB-231, HeLa, MCF-7 and OAW-42 cancer cell lines and also exhibited antimicrobial activities against gram-positive, gram-negative bacteria and fungi. Compound 1 recorded significant antibacterial activity against Xanthomonas campestris and Escherichia coli (8 μg/ml and compound 2 presented highest activity against Bacillus subtilis (4 μg/ml. Compounds 1 and 2 were active against pathogenic fungi to plants and human beings. The activity was compared with griseofulvin and amphotericin-B, which are standard fungicides. The activity of 16 μg/ml by compound 1 was recorded against Epidermophyton floccosum; an anthropophilic dermatophyte responsible for tinea pedis, tinea cruris and tinea corporis. To the best of our knowledge this is the first narration on the isolation of supra said compounds from the genus Pseudonocardia.

  7. Preparation and biocompatibility evaluation of apatite/wollastonite-derived porous bioactive glass ceramic scaffolds

    International Nuclear Information System (INIS)

    Zhang Hua; Ye Xiaojian; Li Jiashun

    2009-01-01

    An apatite/wollastonite-derived (A/W) porous glass ceramic scaffold with highly interconnected pores was successfully fabricated by adding a plastic porosifier. The morphology, porosity and mechanical strength were characterized. The results showed that the glass ceramic scaffold with controllable pore size and porosity displayed open macropores. In addition, good in vitro bioactivity was found for the scaffold obtained by soaking it in simulated body fluid. Mesenchymal stem cells (MSCs) were cultured, expanded and seeded on the scaffold, and the adhesion and proliferation of MSCs were determined using MTT assay and environmental scanning electron microscopy (ESEM). The results revealed that the scaffold was biocompatible and had no negative effects on the MSCs in vitro. The in vivo biocompatibility and osteogenicity were investigated by implanting both the pure scaffold and the MSC/scaffold construct in rabbit mandibles and studying histologically. The results showed that the glass ceramic scaffold exhibited good biocompatibility and osteoconductivity. Moreover, the introduction of MSCs into the scaffold observably improved the efficiency of new bone formation, especially at the initial stage after implantation. However, the glass ceramic scaffold showed the same good biocompatibility and osteogenicity as the hybrid one at the later stage. These results indicate that porous bioactive scaffolds based on the original apatite-wollastonite glass ceramic fulfil the basic requirements of a bone tissue engineering scaffold.

  8. Bioactive Compounds Derived from the Yeast Metabolism of Aromatic Amino Acids during Alcoholic Fermentation

    Directory of Open Access Journals (Sweden)

    Albert Mas

    2014-01-01

    Full Text Available Metabolites resulting from nitrogen metabolism in yeast are currently found in some fermented beverages such as wine and beer. Their study has recently attracted the attention of researchers. Some metabolites derived from aromatic amino acids are bioactive compounds that can behave as hormones or even mimic their role in humans and may also act as regulators in yeast. Although the metabolic pathways for their formation are well known, the physiological significance is still far from being understood. The understanding of this relevance will be a key element in managing the production of these compounds under controlled conditions, to offer fermented food with specific enrichment in these compounds or even to use the yeast as nutritional complements.

  9. New Metabolites and Bioactive Chlorinated Benzophenone Derivatives Produced by a Marine-Derived Fungus Pestalotiopsis heterocornis

    Directory of Open Access Journals (Sweden)

    Hui Lei

    2017-03-01

    Full Text Available Four new compounds, including two isocoumarins, pestaloisocoumarins A and B (1, 2, one sesquiterpenoid degradation, isopolisin B (4, and one furan derivative, pestalotiol A (5, together with one known isocoumarin, gamahorin (3, and three chlorinated benzophenone derivatives, pestalachloride B (6, pestalachloride E (7 and a mixture of pestalalactone atropisomers (8a/8b, were isolated from a culture of the fungus Pestalotiopsis heterocornis associated with sponge Phakellia fusca. These new chemical structures were established using NMR and MS spectroscopic data, as well as single-crystal X-ray crystallographic analysis and CD Cotton effects. All of the isolated compounds were evaluated for their antimicrobial and cytotoxic activities. Isocoumarins 1–3, showed antibacterial activities against Gram-positive bacteria Staphylococcus aureus and Bacillus subtilis with MIC values ranging from 25 to 100 μg/mL and weak antifungal activities. Chlorinated benzophenone derivatives 6–8 exhibited antibacterial activities against S. aureus and B. subtilis with MIC values ranging from 3.0 to 50 μg/mL and cytotoxicities against four human cancer cell lines with IC50 values of 6.8–87.8 μM.

  10. Cell factory-derived bioactive molecules with polymeric cryogel scaffold enhance the repair of subchondral cartilage defect in rabbits.

    Science.gov (United States)

    Gupta, Ankur; Bhat, Sumrita; Chaudhari, Bhushan P; Gupta, Kailash C; Tägil, Magnus; Zheng, Ming Hao; Kumar, Ashok; Lidgren, Lars

    2017-06-01

    We have explored the potential of cell factory-derived bioactive molecules, isolated from conditioned media of primary goat chondrocytes, for the repair of subchondral cartilage defects. Enzyme-linked immunosorbent assay (ELISA) confirms the presence of transforming growth factor-β1 in an isolated protein fraction (12.56 ± 1.15 ng/mg protein fraction). These bioactive molecules were used alone or with chitosan-agarose-gelatin cryogel scaffolds, with and without chondrocytes, to check whether combined approaches further enhance cartilage repair. To evaluate this, an in vivo study was conducted on New Zealand rabbits in which a subchondral defect (4.5 mm wide × 4.5 mm deep) was surgically created. Starting after the operation, bioactive molecules were injected at the defect site at regular intervals of 14 days. Histopathological analysis showed that rabbits treated with bioactive molecules alone had cartilage regeneration after 4 weeks. However, rabbits treated with bioactive molecules along with scaffolds, with or without cells, showed cartilage formation after 3 weeks; 6 weeks after surgery, the cartilage regenerated in rabbits treated with either bioactive molecules alone or in combinations showed morphological similarities to native cartilage. No systemic cytotoxicity or inflammatory response was induced by any of the treatments. Further, ELISA was done to determine systemic toxicity, which showed no difference in concentration of tumour necrosis factor-α in blood serum, before or after surgery. In conclusion, intra-articular injection with bioactive molecules alone may be used for the repair of subchondral cartilage defects, and bioactive molecules along with chondrocyte-seeded scaffolds further enhance the repair. Copyright © 2015 John Wiley & Sons, Ltd. Copyright © 2015 John Wiley & Sons, Ltd.

  11. Bioactive Phenylalanine Derivatives and Cytochalasins from the Soft Coral-Derived Fungus, Aspergillus elegans

    Directory of Open Access Journals (Sweden)

    Xue-Ping Sun

    2013-06-01

    Full Text Available One new phenylalanine derivative 4′-OMe-asperphenamate (1, along with one known phenylalanine derivative (2 and two new cytochalasins, aspochalasin A1 (3 and cytochalasin Z24 (4, as well as eight known cytochalasin analogues (5–12 were isolated from the fermentation broth of Aspergillus elegans ZJ-2008010, a fungus obtained from a soft coral Sarcophyton sp. collected from the South China Sea. Their structures and the relative configurations were elucidated using comprehensive spectroscopic methods. The absolute configuration of 1 was determined by chemical synthesis and Marfey’s method. All isolated metabolites (1–12 were evaluated for their antifouling and antibacterial activities. Cytochalasins 5, 6, 8 and 9 showed strong antifouling activity against the larval settlement of the barnacle Balanus amphitrite, with the EC50 values ranging from 6.2 to 37 μM. This is the first report of antifouling activity for this class of metabolites. Additionally, 8 exhibited a broad spectrum of antibacterial activity, especially against four pathogenic bacteria Staphylococcus albus, S. aureus, Escherichia coli and Bacillus cereus.

  12. Elucidating the biosynthetic and regulatory mechanisms of flavonoid-derived bioactive components in Epimedium sagittatum

    Directory of Open Access Journals (Sweden)

    Wenjun eHuang

    2015-09-01

    Full Text Available Herba epimedii (Epimedium, a traditional Chinese medicine, has been widely used as a kidney tonic and antirheumatic medicine for thousands of years. In Epimedium, flavonoids have been demonstrated to be the main bioactive components (BCs. However, the molecular biosynthetic and regulatory mechanisms of flavonoid-derived BCs remain obscure. In this study, we isolated twelve structural genes and two putative transcription factors (TFs in the flavonoid pathway. Phytochemical analysis showed that the total content of four representative BCs (epimedin A, B, C and icariin decreased slightly or dramatically in two lines of E. sagittatum during leaf development. Transcriptional analysis revealed that two R2R3-MYB TFs (EsMYBA1 and EsMYBF1, together with a bHLH TF (EsGL3 and WD40 protein (EsTTG1, were supposed to coordinately regulate the anthocyanin and flavonol-derived BCs biosynthesis in leaves. Overexpression of EsFLS (flavonol synthase in tobacco resulted in increased flavonols content and decreased anthocyanins content in flowers. Moreover, EsMYB12 negatively correlated with the accumulation of the four BCs, and might act as a transcriptional repressor in the flavonoid pathway. Therefore, the anthocyanin pathway may coordinate with the flavonol-derived BCs pathway in Epimedium leaves. A better understanding of the flavonoid biosynthetic and regulatory mechanisms in E. sagittatum will facilitate functional characterization, metabolic engineering and molecular breeding studies of Epimedium species.

  13. Stamen-derived bioactive gibberellin is essential for male flower development of Cucurbita maxima L.

    Science.gov (United States)

    Pimenta Lange, Maria João; Knop, Nicole; Lange, Theo

    2012-04-01

    Gibberellin (GA) signalling during pumpkin male flower development is highly regulated, including biosynthetic, perception, and transduction pathways. GA 20-oxidases, 3-oxidases, and 2-oxidases catalyse the final part of GA synthesis. Additionally, 7-oxidase initiates this part of the pathway in some cucurbits including Cucurbita maxima L. (pumpkin). Expression patterns for these GA-oxidase-encoding genes were examined by competitive reverse transcription-PCR (RT-PCR) and endogenous GA levels were determined during pumpkin male flower development. In young flowers, GA20ox3 transcript levels are high in stamens, followed by high levels of the GA precursor GA(9). Later, just before flower opening, transcript levels for GA3ox3 and GA3ox4 increase in the hypanthium and stamens, respectively. In the stamen, following GA3ox4 expression, bioactive GA(4) levels rise dramatically. Accordingly, catabolic GA2ox2 and GA2ox3 transcript levels are low in developing flowers, and increase in mature flowers. Putative GA receptor GID1b and DELLA repressor GAIPb transcript levels do not change in developing flowers, but increase sharply in mature flowers. Emasculation arrests floral development completely and leads to abscission of premature flowers. Application of GA(4) (but not of its precursors GA(12)-aldehyde or GA(9)) restores normal growth of emasculated flowers. These results indicate that de novo GA(4) synthesis in the stamen is under control of GA20ox3 and GA3ox4 genes just before the rapid flower growth phase. Stamen-derived bioactive GA is essential and sufficient for male flower development, including the petal and the pedicel growth.

  14. Influence of Cu doping in borosilicate bioactive glass and the properties of its derived scaffolds.

    Science.gov (United States)

    Wang, Hui; Zhao, Shichang; Xiao, Wei; Xue, Jingzhe; Shen, Youqu; Zhou, Jie; Huang, Wenhai; Rahaman, Mohamed N; Zhang, Changqing; Wang, Deping

    2016-01-01

    Copper doped borosilicate glasses (BG-Cu) were studied by means of FT-IR, Raman, UV-vis and NMR spectroscopies to investigate the changes that appeared in the structure of borosilicate glass matrix by doping copper ions. Micro-fil and immunohistochemistry analysis were applied to study the angiogenesis of its derived scaffolds in vivo. Results indicated that the Cu ions significantly increased the B-O bond of BO4 groups at 980 cm(-1), while they decrease that of BO2O(-) groups at 1440-1470 cm(-1) as shown by Raman spectra. A negative shift was observed from (11)B and (29)Si NMR spectra. The (11)B NMR spectra exhibited a clear transformation from BO3 into BO4 groups, caused by the agglutination effect of the Cu ions and the charge balance of the agglomerate in the glass network, leading to a more stable glass network and lower ions release rate in the degradation process. Furthermore, the BG-Cu scaffolds significantly enhanced blood vessel formation in rat calvarial defects at 8 weeks post-implantation. Generally, it suggested that the introduction of Cu into borosilicate glass endowed glass and its derived scaffolds with good properties, and the cooperation of Cu with bioactive glass may pave a new way for tissue engineering. Copyright © 2015 Elsevier B.V. All rights reserved.

  15. Protein-tannic acid multilayer films: A multifunctional material for microencapsulation of food-derived bioactives.

    Science.gov (United States)

    Lau, Hooi Hong; Murney, Regan; Yakovlev, Nikolai L; Novoselova, Marina V; Lim, Su Hui; Roy, Nicole; Singh, Harjinder; Sukhorukov, Gleb B; Haigh, Brendan; Kiryukhin, Maxim V

    2017-11-01

    The benefits of various functional foods are often negated by stomach digestion and poor targeting to the lower gastrointestinal tract. Layer-by-Layer assembled protein-tannic acid (TA) films are suggested as a prospective material for microencapsulation of food-derived bioactive compounds. Bovine serum albumin (BSA)-TA and pepsin-TA films demonstrate linear growth of 2.8±0.1 and 4.2±0.1nm per bi-layer, correspondingly, as shown by ellipsometry. Both multilayer films are stable in simulated gastric fluid but degrade in simulated intestinal fluid. Their corresponding degradation constants are 0.026±0.006 and 0.347±0.005nm -1 min -1 . Milk proteins possessing enhanced adhesion to human intestinal surface, Immunoglobulin G (IgG) and β-Lactoglobulin (BLG), are explored to tailor targeting function to BSA-TA multilayer film. BLG does not adsorb onto the multilayer while IgG is successfully incorporated. Microcapsules prepared from the multilayer demonstrate 2.7 and 6.3 times higher adhesion to Caco-2 cells when IgG is introduced as an intermediate and the terminal layer, correspondingly. This developed material has a great potential for oral delivery of numerous active food-derived ingredients. Copyright © 2017 Elsevier Inc. All rights reserved.

  16. Sol-gel derived bioactive coating on zirconia: Effect on flexural strength and cell proliferation.

    Science.gov (United States)

    Shahramian, Khalil; Leminen, Heidi; Meretoja, Ville; Linderbäck, Paula; Kangasniemi, Ilkka; Lassila, Lippo; Abdulmajeed, Aous; Närhi, Timo

    2017-11-01

    The purpose of this study was to evaluate the effect of sol-gel derived bioactive coatings on the biaxial flexural strength and fibroblast proliferation of zirconia, aimed to be used as an implant abutment material. Yttrium stabilized zirconia disc-shaped specimens were cut, ground, sintered, and finally cleansed ultrasonically in each of acetone and ethanol for 5 minutes. Three experimental groups (n = 15) were fabricated, zirconia with sol-gel derived titania (TiO 2 ) coating, zirconia with sol-gel derived zirconia (ZrO 2 ) coating, and non-coated zirconia as a control. The surfaces of the specimens were analyzed through images taken using a scanning electron microscope (SEM), and a non-contact tapping mode atomic force microscope (AFM) was used to record the surface topography and roughness of the coated specimens. Biaxial flexural strength values were determined using the piston-on-three ball technique. Human gingival fibroblast proliferation on the surface of the specimens was evaluated using AlamarBlue assay™. Data were analyzed using a one-way analysis of variance (ANOVA) followed by Tukey's post-hoc test. Additionally, the biaxial flexural strength data was also statistically analyzed with the Weibull distribution. The biaxial flexural strength of zirconia specimens was unaffected (p > 0.05). Weibull modulus of TiO 2 coated and ZrO 2 coated groups (5.7 and 5.4, respectively) were lower than the control (8.0). Specimens coated with ZrO 2 showed significantly lower fibroblast proliferation compared to other groups (p sol-gel derived coatings have no influence on the flexural strength of zirconia. ZrO 2 coated specimens showed significantly lower cell proliferation after 12 days than TiO 2 coated or non-coated control. © 2016 Wiley Periodicals, Inc. J Biomed Mater Res Part B: Appl Biomater, 105B: 2401-2407, 2017. © 2016 Wiley Periodicals, Inc.

  17. Bioprospecting Chemical Diversity and Bioactivity in a Marine Derived Aspergillus terreus.

    Science.gov (United States)

    Adpressa, Donovon A; Loesgen, Sandra

    2016-02-01

    A comparative metabolomic study of a marine derived fungus (Aspergillus terreus) grown under various culture conditions is presented. The fungus was grown in eleven different culture conditions using solid agar, broth cultures, or grain based media (OSMAC). Multivariate analysis of LC/MS data from the organic extracts revealed drastic differences in the metabolic profiles and guided our subsequent isolation efforts. The compound 7-desmethylcitreoviridin was isolated and identified, and is fully described for the first time. In addition, 16 known fungal metabolites were also isolated and identified. All compounds were elucidated by detailed spectroscopic analysis and tested for antibacterial activities against five human pathogens and tested for cytotoxicity. This study demonstrates that LC/MS based multivariate analysis provides a simple yet powerful tool to analyze the metabolome of a single fungal strain grown under various conditions. This approach allows environmentally-induced changes in metabolite expression to be rapidly visualized, and uses these differences to guide the discovery of new bioactive molecules. Copyright © 2016 Verlag Helvetica Chimica Acta AG, Zürich.

  18. Effect of a bioactive curcumin derivative on DPPC membrane: A DSC and Raman spectroscopy study

    Energy Technology Data Exchange (ETDEWEB)

    Gardikis, Kostantinos [Department of Pharm. Technology, School of Pharmacy, University of Athens, Athens (Greece); Hatziantoniou, Sophia [Department of Pharm. Technology, School of Pharmacy, University of Athens, Athens (Greece); Viras, Kyriakos [Laboratory of Physical Chemistry, Department of Chemistry, University of Athens, Athens (Greece); Demetzos, Costas [Department of Pharm. Technology, School of Pharmacy, University of Athens, Athens (Greece)]. E-mail: demetzos@pharm.uoa.gr

    2006-08-01

    Interactions of dimethoxycurcumin (1) a lipophilic bioactive curcumin derivative with dipalmitoyl phosphatidylcholine (DPPC) were investigated. The thermodynamic changes caused by (1) and its location into DPPC lipid bilayers were monitored by differential scanning calorimetry and Raman spectroscopy. The results reveal that (1) influences the thermotropic properties of DPPC lipid membrane causing abolition of the pretransition and broadening of the phase-transition profile and slightly decreases the T {sub m} at increasing concentrations. The Raman height intensity ratios of the peaks I {sub 2935/2880}, I {sub 2844/2880} and I {sub 1090/1130} are representative of the interaction of (1) with the alkyl chains and furnish information about the ratio between disorder and order that exists in the conformation of the alkyl chain. The intensity changes of the peak at 715 cm{sup -1} indicates interaction between the choline head group and (1). The Raman spectroscopy results are in agreement with the thermal analysis results. Biologically active lipophilic molecules such as (1) should be studied in terms of their interaction with lipid bilayers prior to the development of advanced lipid carrier systems such as liposomes. The results of these studies provide information on the membrane integrity and physicochemical properties that are essential for the rational design lipidic drug delivery systems.

  19. Influence of Cu doping in borosilicate bioactive glass and the properties of its derived scaffolds

    Energy Technology Data Exchange (ETDEWEB)

    Wang, Hui [School of Materials Science and Engineering, Tongji University, Shanghai 2001804 (China); Zhao, Shichang [Department of Orthopedic Surgery, Shanghai Sixth People' s Hospital, Shanghai Jiao Tong University, Shanghai 200233 (China); Xiao, Wei [Department of Materials Science and Engineering, and Center for Biomedical Science and Engineering, Missouri University of Science and Technology, Rolla, MO 65409-0340 (United States); Xue, Jingzhe [Department of Chemistry, Tongji University, Shanghai 200092 (China); Shen, Youqu [Department of Materials Science and Engineering, and Center for Biomedical Science and Engineering, Missouri University of Science and Technology, Rolla, MO 65409-0340 (United States); Zhou, Jie; Huang, Wenhai [School of Materials Science and Engineering, Tongji University, Shanghai 2001804 (China); Rahaman, Mohamed N. [Department of Materials Science and Engineering, and Center for Biomedical Science and Engineering, Missouri University of Science and Technology, Rolla, MO 65409-0340 (United States); Zhang, Changqing, E-mail: shzhangchangqing@163.com [Department of Orthopedic Surgery, Shanghai Sixth People' s Hospital, Shanghai Jiao Tong University, Shanghai 200233 (China); Wang, Deping, E-mail: wdpshk@tongji.edu.cn [School of Materials Science and Engineering, Tongji University, Shanghai 2001804 (China)

    2016-01-01

    Copper doped borosilicate glasses (BG–Cu) were studied by means of FT-IR, Raman, UV–vis and NMR spectroscopies to investigate the changes that appeared in the structure of borosilicate glass matrix by doping copper ions. Micro-fil and immunohistochemistry analysis were applied to study the angiogenesis of its derived scaffolds in vivo. Results indicated that the Cu ions significantly increased the B–O bond of BO{sub 4} groups at 980 cm{sup −1}, while they decrease that of BO{sub 2}O{sup −} groups at 1440–1470 cm{sup −1} as shown by Raman spectra. A negative shift was observed from {sup 11}B and {sup 29}Si NMR spectra. The {sup 11}B NMR spectra exhibited a clear transformation from BO{sub 3} into BO{sub 4} groups, caused by the agglutination effect of the Cu ions and the charge balance of the agglomerate in the glass network, leading to a more stable glass network and lower ions release rate in the degradation process. Furthermore, the BG–Cu scaffolds significantly enhanced blood vessel formation in rat calvarial defects at 8 weeks post-implantation. Generally, it suggested that the introduction of Cu into borosilicate glass endowed glass and its derived scaffolds with good properties, and the cooperation of Cu with bioactive glass may pave a new way for tissue engineering. - Highlights: • Agglutination effect of Cu{sup 2+} and charge balance of agglomerate lead to more stable glass. • Lower degradability and lower ions release were found in BG-Cu scaffolds. • Excellent angiogenesis and sustain Cu{sup 2+} release were endowed by doping Cu.

  20. Photocurable bioactive bone cement based on hydroxyethyl methacrylate-poly(acrylic/maleic) acid resin and mesoporous sol gel-derived bioactive glass

    Energy Technology Data Exchange (ETDEWEB)

    Hesaraki, S., E-mail: S-hesaraki@merc.ac.ir

    2016-06-01

    This paper reports on strong and bioactive bone cement based on ternary bioactive SiO{sub 2}-CaO-P{sub 2}O{sub 5} glass particles and a photocurable resin comprising hydroxyethyl methacrylate (HEMA) and poly(acrylic/maleic) acid. The as-cured composite represented a compressive strength of about 95 MPa but it weakened during soaking in simulated body fluid, SBF, qua its compressive strength reached to about 20 MPa after immersing for 30 days. Biodegradability of the composite was confirmed by reducing its initial weight (~ 32%) as well as decreasing the molecular weight of early cured resin during the soaking procedure. The composite exhibited in vitro calcium phosphate precipitation in the form of nanosized carbonated hydroxyapatite, which indicates its bone bonding ability. Proliferation of calvarium-derived newborn rat osteoblasts seeded on top of the composite was observed during incubation at 37 °C, meanwhile, an adequate cell supporting ability was found. Consequently, it seems that the produced composite is an appropriate alternative for bone defect injuries, because of its good cell responses, high compressive strength and ongoing biodegradability, though more in vivo experiments are essential to confirm this assumption. - Highlights: • Light cure cement based on SiO{sub 2}-CaO-P{sub 2}O{sub 5} glass and polymer-like matrix was formed. • The matrix includes poly(acrylic/maleic acid) and poly(hydroxyethyl methacrylate). • The cement is as strong as polymethylmethacrylate bone cement. • The cement exhibits apatite formation ability in simulated body fluid. • The cement is biodegradable and supports proliferation of osteoblastic cells.

  1. Bioactivity of immobilized hyaluronic acid derivatives regarding protein adsorption and cell adhesion

    DEFF Research Database (Denmark)

    Köwitsch, Alexander; Yang, Yuan; Ma, Ning

    2011-01-01

    with HA on physicochemical surface properties of these substrata and estimates of the quantities of immobilized HA were obtained by different physical methods such as contact angle measurements, ellipsometry, and atomic force microscopy. The bioactivity of aHA and tHA toward their natural binding partner...... affects cell growth and differentiation. A lower number and spreading of cells were observed on HA-modified surfaces compared to amino- and vinyl-terminated glass and silicon surfaces. Immunofluorescence microscopy also revealed that adhesion of fibroblast plated on HA-modified surfaces was mediated...... primarily by HA receptor CD44, indicating that bioactivity of HA was not significantly reduced by chemical modification....

  2. Biocompatibility and bioactivity of porous polymer-derived Ca-Mg silicate ceramics.

    Science.gov (United States)

    Fiocco, L; Li, S; Stevens, M M; Bernardo, E; Jones, J R

    2017-03-01

    Magnesium is a trace element in the human body, known to have important effects on cell differentiation and the mineralisation of calcified tissues. This study aimed to synthesise highly porous Ca-Mg silicate foamed scaffolds from preceramic polymers, with analysis of their biological response. Akermanite (Ak) and wollastonite-diopside (WD) ceramic foams were obtained from the pyrolysis of a liquid silicone mixed with reactive fillers. The porous structure was obtained by controlled water release from selected fillers (magnesium hydroxide and borax) at 350°C. The homogeneous distribution of open pores, with interconnects of modal diameters of 160-180μm was obtained and maintained after firing at 1100°C. Foams, with porosity exceeding 80%, exhibited compressive strength values of 1-2MPa. In vitro studies were conducted by immersion in SBF for 21days, showing suitable dissolution rates, pH and ionic concentrations. Cytotoxicity analysis performed in accordance with ISO10993-5 and ISO10993-12 standards confirmed excellent biocompatibility of both Ak and WD foams. In addition, MC3T3-E1 cells cultured on the Mg-containing scaffolds demonstrated enhanced osteogenic differentiation and the expression of osteogenic markers including Collagen Type I, Osteopontin and Osteocalcin, in comparison to Mg-free counterparts. The results suggest that the addition of magnesium can further enhance the bioactivity and the potential for bone regeneration applications of Ca-silicate materials. Here, we show that the incorporation of Mg in Ca-silicates plays a significant role in the enhancement of the osteogenic differentiation and matrix formation of MC3T3-E1 cells, cultured on polymer-derived highly porous scaffolds. Reduced degradation rates and improved mechanical properties are also observed, compared to Mg-free counterparts, suggesting the great potential of Ca-Mg silicates as bone tissue engineering materials. Excellent biocompatibility of the new materials, in accordance to

  3. Feasibility Study of a Standardized Novel Animal Model for Cervical Vertebral Augmentation in Sheep Using a PTH Derivate Bioactive Material

    Directory of Open Access Journals (Sweden)

    Karina Klein

    2014-08-01

    Full Text Available Prophylactic local treatment involving percutaneous vertebral augmentation using bioactive materials is a new treatment strategy in spine surgery in humans for vertebral bodies at risk. Standardized animal models for this procedure are almost non-existent. The purpose of this study was to: (i prove the efficacy of PTH derivate bioactive materials for new bone formation; and (ii create a new, highly standardized cervical vertebral augmentation model in sheep. Three different concentrations of a modified form of parathyroid hormone (PTH covalently bound to a fibrin matrix containing strontium carbonate were used. The same matrix without PTH and shams were used as controls. The bioactive materials were locally injected. Using a ventral surgical approach, a pre-set amount of material was injected under fluoroscopic guidance into the intertrabecular space of three vertebral bodies. Intravital fluorescent dyes were used to demonstrate new bone formation. After an observation period of four months, the animals were sacrificed, and vertebral bodies were processed for µCT, histomorphometry, histology and sequential fluorescence evaluation. Enhanced localized bone activity and new bone formation in the injected area could be determined for all experimental groups in comparison to the matrix alone and sham with the highest values detected for the group with a medium concentration of PTH.

  4. The Fabrication and Characterization of PCL/Rice Husk Derived Bioactive Glass-Ceramic Composite Scaffolds

    Directory of Open Access Journals (Sweden)

    Farnaz Naghizadeh

    2014-01-01

    Full Text Available The present study was conducted to fabricate a 3D scaffold using polycaprolactone (PCL and silicate based bioactive glass-ceramic (R-SBgC. Different concentrations of R-SBgC prepared from rice husk ash (RHA were combined with PCL to fabricate a composite scaffold using thermally induced phase separation (TIPS method. The products were then characterized using SEM and EDX. The results demonstrated that R-SBgC in PCL matrix produced a bioactive material which has highly porous structure with interconnected porosities. There appears to be a relationship between the increase in R-SBgC concentration and increased material density and compressive modulus; however, increasing R-SBgC concentration result in reduced scaffold porosity. In conclusion, it is possible to fabricate a PCL/bioactive glass-ceramic composite from processed rice husk. Varying the R-SBgC concentrations can control the properties of this material, which is useful in the development of the ideal scaffold intended for use as a bone substitute in nonload bearing sites.

  5. Discovery Strategies of Bioactive Compounds Synthesized by Nonribosomal Peptide Synthetases and Type-I Polyketide Synthases Derived from Marine Microbiomes

    Science.gov (United States)

    Amoutzias, Grigoris D.; Chaliotis, Anargyros; Mossialos, Dimitris

    2016-01-01

    Considering that 70% of our planet’s surface is covered by oceans, it is likely that undiscovered biodiversity is still enormous. A large portion of marine biodiversity consists of microbiomes. They are very attractive targets of bioprospecting because they are able to produce a vast repertoire of secondary metabolites in order to adapt in diverse environments. In many cases secondary metabolites of pharmaceutical and biotechnological interest such as nonribosomal peptides (NRPs) and polyketides (PKs) are synthesized by multimodular enzymes named nonribosomal peptide synthetases (NRPSes) and type-I polyketide synthases (PKSes-I), respectively. Novel findings regarding the mechanisms underlying NRPS and PKS evolution demonstrate how microorganisms could leverage their metabolic potential. Moreover, these findings could facilitate synthetic biology approaches leading to novel bioactive compounds. Ongoing advances in bioinformatics and next-generation sequencing (NGS) technologies are driving the discovery of NRPs and PKs derived from marine microbiomes mainly through two strategies: genome-mining and metagenomics. Microbial genomes are now sequenced at an unprecedented rate and this vast quantity of biological information can be analyzed through genome mining in order to identify gene clusters encoding NRPSes and PKSes of interest. On the other hand, metagenomics is a fast-growing research field which directly studies microbial genomes and their products present in marine environments using culture-independent approaches. The aim of this review is to examine recent developments regarding discovery strategies of bioactive compounds synthesized by NRPS and type-I PKS derived from marine microbiomes and to highlight the vast diversity of NRPSes and PKSes present in marine environments by giving examples of recently discovered bioactive compounds. PMID:27092515

  6. Discovery Strategies of Bioactive Compounds Synthesized by Nonribosomal Peptide Synthetases and Type-I Polyketide Synthases Derived from Marine Microbiomes

    Directory of Open Access Journals (Sweden)

    Grigoris D. Amoutzias

    2016-04-01

    Full Text Available Considering that 70% of our planet’s surface is covered by oceans, it is likely that undiscovered biodiversity is still enormous. A large portion of marine biodiversity consists of microbiomes. They are very attractive targets of bioprospecting because they are able to produce a vast repertoire of secondary metabolites in order to adapt in diverse environments. In many cases secondary metabolites of pharmaceutical and biotechnological interest such as nonribosomal peptides (NRPs and polyketides (PKs are synthesized by multimodular enzymes named nonribosomal peptide synthetases (NRPSes and type-I polyketide synthases (PKSes-I, respectively. Novel findings regarding the mechanisms underlying NRPS and PKS evolution demonstrate how microorganisms could leverage their metabolic potential. Moreover, these findings could facilitate synthetic biology approaches leading to novel bioactive compounds. Ongoing advances in bioinformatics and next-generation sequencing (NGS technologies are driving the discovery of NRPs and PKs derived from marine microbiomes mainly through two strategies: genome-mining and metagenomics. Microbial genomes are now sequenced at an unprecedented rate and this vast quantity of biological information can be analyzed through genome mining in order to identify gene clusters encoding NRPSes and PKSes of interest. On the other hand, metagenomics is a fast-growing research field which directly studies microbial genomes and their products present in marine environments using culture-independent approaches. The aim of this review is to examine recent developments regarding discovery strategies of bioactive compounds synthesized by NRPS and type-I PKS derived from marine microbiomes and to highlight the vast diversity of NRPSes and PKSes present in marine environments by giving examples of recently discovered bioactive compounds.

  7. Sol-gel derived manganese-releasing bioactive glass as a therapeutical approach for bone tissue engineering

    Energy Technology Data Exchange (ETDEWEB)

    Barrioni, B.R.; Oliveira, A.C.; Leite, M.F.; Pereira, M.M. [Universidade Federal de Minas Gerais (UFMG), MG (Brazil)

    2016-07-01

    Full text: Bioactive glasses (BG) have been highlighted in tissue engineering, due to their high bioactivity and biocompatibility, being potential materials for bone tissue repair. Its composition is variable and quite flexible, allowing the incorporation of therapeutic metallic ions, which has been regarded as a promising approach in the development of BG with superior properties for tissue engineering. These ions can be released in a controlled manner during the dissolution process of the glass, having the advantage of being released at the exactly implant site where they are needed, thus optimizing the therapeutic efficacy and reducing undesired side effects in the patient. Among several ions that have been studied, Manganese (Mn) has been shown to favor osteogenic differentiation. Besides, this ion is also a cofactor for several enzymes involved in remodeling of extracellular matrix, presenting an important role in cell adhesion. Therefore, it is very important to study the Mn role in the BG network and its influence on the glass bioactivity. In this context, new bioactive glass compositions derived from the 58S (60%SiO2-36%CaO-4%P2O5, mol%) were synthesized in this work, using the sol-gel method, by the incorporation of Mn into their structure. FTIR and Raman spectra showed the presence of typical BG chemical groups, whereas the amorphous structure typical of these materials was confirmed by XRD analysis, which also indicated that the Mn incorporation in the glass network was well succeeded, as its precursor did not recrystallize. The role of Mn in the glass network was also evaluated by XPS. The influence of Mn on carbonated hydroxyapatite layer formation after different periods of immersion of the BG powder in Simulated Body Fluid was evaluated using zeta potential, SEM, EDS and FTIR, whereas the controlled ion release was measured through ICP-OES. MTT assay revealed that Mn-containing BG showed no cytotoxic effect on cell culture. All these results indicate

  8. Sol-gel derived manganese-releasing bioactive glass as a therapeutical approach for bone tissue engineering

    International Nuclear Information System (INIS)

    Barrioni, B.R.; Oliveira, A.C.; Leite, M.F.; Pereira, M.M.

    2016-01-01

    Full text: Bioactive glasses (BG) have been highlighted in tissue engineering, due to their high bioactivity and biocompatibility, being potential materials for bone tissue repair. Its composition is variable and quite flexible, allowing the incorporation of therapeutic metallic ions, which has been regarded as a promising approach in the development of BG with superior properties for tissue engineering. These ions can be released in a controlled manner during the dissolution process of the glass, having the advantage of being released at the exactly implant site where they are needed, thus optimizing the therapeutic efficacy and reducing undesired side effects in the patient. Among several ions that have been studied, Manganese (Mn) has been shown to favor osteogenic differentiation. Besides, this ion is also a cofactor for several enzymes involved in remodeling of extracellular matrix, presenting an important role in cell adhesion. Therefore, it is very important to study the Mn role in the BG network and its influence on the glass bioactivity. In this context, new bioactive glass compositions derived from the 58S (60%SiO2-36%CaO-4%P2O5, mol%) were synthesized in this work, using the sol-gel method, by the incorporation of Mn into their structure. FTIR and Raman spectra showed the presence of typical BG chemical groups, whereas the amorphous structure typical of these materials was confirmed by XRD analysis, which also indicated that the Mn incorporation in the glass network was well succeeded, as its precursor did not recrystallize. The role of Mn in the glass network was also evaluated by XPS. The influence of Mn on carbonated hydroxyapatite layer formation after different periods of immersion of the BG powder in Simulated Body Fluid was evaluated using zeta potential, SEM, EDS and FTIR, whereas the controlled ion release was measured through ICP-OES. MTT assay revealed that Mn-containing BG showed no cytotoxic effect on cell culture. All these results indicate

  9. Hydroxylated phenylacetamides derived from bioactive benzoxazinoids are bioavailable in humans after habitual consumption of whole grain sourdough rye bread.

    Science.gov (United States)

    Beckmann, Manfred; Lloyd, Amanda J; Haldar, Sumanto; Seal, Chris; Brandt, Kirsten; Draper, John

    2013-10-01

    Understanding relationships between dietary whole grain and health is hindered by incomplete knowledge of potentially bioactive metabolites derived from these foods. We aimed to discover compounds in urine correlated with changes in amounts of whole grain rye consumption. After a wash-out period, volunteers consumed 48-g whole grain rye foods per day for 4 wk and then doubled their intake for a further 4 wk. Samples of 24-h urines were analyzed by flow infusion electrospray MS followed by supervised multivariate data analysis. Urine samples from participants who reported high intakes of rye flakes, rye pasta, or total whole grain rye products could not be discriminated adequately from their wash-out samples. However, discrimination was seen in urine samples from participants who reported high whole grain sourdough rye bread consumption. Accurate mass analysis of explanatory signals followed by fragmentation identified conjugates of the benzoxazinoid lactam 2-hydroxy-1,4-benzoxazin-3-one and hydroxylated phenyl acetamide derivatives. Statistical validation showed sensitivities of 84-96% and specificities of 70-81% (p values bread consumption. Several potentially bioactive alkaloids have been identified in humans consuming fermented whole grain sourdough rye bread. © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

  10. Dihydroresveratrol Type Dihydrostilbenoids: Chemical Diversity, Chemosystematics, and Bioactivity.

    Science.gov (United States)

    Vitalini, Sara; Cicek, Serhat S; Granica, Sebastian; Zidorn, Christian

    2018-01-01

    Dihydrostilbenoids, a diverse class of natural products differing from stilbenoids by the missing double bond in the ethylene chain linking the aromatic moieties, have been reported from fungi, mosses, ferns, and flowering plants. Occurrence, structure, and bioactivity of naturally occurring dihydroresveratrol type dihydrostilbenoids are discussed in this review. A Reaxys database search for dihydroresveratrol derivatives with possible substitutions on all atoms, but excluding non-natural products and compounds featuring additional rings involving the ethyl connecting chain, was performed. Structures include simple dihydroresveratrol derivatives, compounds substituted with complex side chains composed of acyl moieties and sugars, and compounds containing polycyclic cores attached to dihydrostilbenoid units. Dihydrostilbenoids have a wide spectrum of bioactivities ranging from expectable antioxidant and anti-inflammatory activities to interesting neuroprotective and anticancer activity. The anticancer activity in particular is very pronounced for some plant-derived dihydrostilbenoids and makes them interesting lead compounds for drug development. Apart from some reports on dihydroresveratrol derivatives as phytoalexins against plant-pathogenic fungi, only very limited information is available on the ecological role of these compounds for the organisms producing them. Dihydrostilbenoids are a class of natural products possessing significant biological activities; their scattered but not ubiquitous occurrence throughout the kingdoms of plants and fungi is not easily explained. We are convinced that future studies will identify new sources of dihydrostilbenoids, and we hope that the present review will inspire such studies and will help in directing such efforts to suitable source organisms and towards promising bioactivities. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

  11. The role of bioactive substances in controlling foodborne pathogens derived from Metasequoia glyptostroboides Miki ex Hu.

    Science.gov (United States)

    Bajpai, Vivek K; Na, Minkyun; Kang, Sun Chul

    2010-07-01

    In an attempt to isolate bioactive substances, ethyl acetate cone extract of Metasequoia glyptostroboides was subjected to a column chromatographic analysis that resulted in isolation of an abietane type diterpenoid, taxoquinone. Its structure was elucidated by spectroscopic means. In further, taxoquinone showed potential antibacterial effect as diameters of zones of inhibition against foodborne pathogenic bacteria such as Listeria monocytogenes ATCC 19166, Salmonella typhimurium KCTC 2515, Salmonella enteritidis KCTC 2021, Escherichia coli ATCC 8739, E. coli O157:H7 ATCC 43888, Enterobacter aerogenes KCTC2190, Staphylococcus aureus ATCC 6538 and S. aureus KCTC 1916, which were found in the range of 10.6-15.8mm. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) values of taxoquinone against the employed bacterial pathogens were found in the range of 62.5-250 and 125-500 microg/ml. Also the compound had strong antibacterial effect on the viable counts of the tested bacteria. Further, scanning electron microscopic study demonstrated potential detrimental effect of taxoquinone on the morphology of E. coli ATCC 8739. These findings indicate that bioactive compound taxoquinone present in M. glyptostroboides could be used as a promising antibacterial agent in food industry to inhibit the growth of certain important foodborne pathogens. 2010 Elsevier Ltd. All rights reserved.

  12. Screening plant derived dietary phenolic compounds for bioactivity related to cardiovascular disease.

    Science.gov (United States)

    Croft, Kevin D; Yamashita, Yoko; O'Donoghue, Helen; Shirasaya, Daishi; Ward, Natalie C; Ashida, Hitoshi

    2018-04-01

    The potential health benefits of phenolic acids found in food and beverages has been suggested from a number of large population studies. However, the mechanism of how these compounds may exert biological effects is less well established. It is also now recognised that many complex polyphenols in the diet are metabolised to simple phenolic acids which can be taken up in the circulation. In this paper a number of selected phenolic compounds have been tested for their bioactivity in two cell culture models. The expression and activity of endothelial nitric oxide synthase (eNOS) in human aortic endothelial cells and the uptake of glucose in muscle cells. Our data indicate that while none of the compounds tested had a significant effect on eNOS expression or activation in endothelial cells, several of the compounds increased glucose uptake in muscle cells. These compounds also enhanced the translocation of the glucose transporter GLUT4 to the plasma membrane, which may explain the observed increase in cellular glucose uptake. These results indicate that simple cell culture models may be useful to help understand the bioactivity of phenolic compounds in relation to cardiovascular protection. Copyright © 2017 Elsevier B.V. All rights reserved.

  13. Bioactive 2(1H-Pyrazinones and Diketopiperazine Alkaloids from a Tunicate-Derived Actinomycete Streptomyces sp.

    Directory of Open Access Journals (Sweden)

    Lamiaa A. Shaala

    2016-08-01

    Full Text Available As a part of our ongoing effort to allocate marine microbial bioactive leads, a tunicate-derived actinomycete, Streptomyces sp. Did-27, was investigated. Three new 2(1H-pyrazinones derivatives, (S-6-(sec-butyl-3-isopropylpyrazin-2(1H-one (1, (S-3-(sec-butyl-6-isopropylpyrazin-2(1H-one (2 and (S-6-(sec-butyl-3-isobutylpyrazin-2(1H-one (3, together with the known (1H-pyrazinones analogues deoxymutaaspergillic acid (4, 3,6-diisobutyl-2(1H-pyrazinone (5 and 3,6-di-sec-butyl-2(1H-pyrazinone (6, and the diketopiperazine alkaloids cyclo(6-OH-d-Pro-l-Phe (7, bacillusamide B (8, cyclo(l-Pro-l-Leu and cyclo(l-Pro-l-Ile (10 were isolated from this strain. The structures of the compounds were determined by study of their one- and two-dimensional NMR spectra as well as high-resolution mass spectral determinations. Compound 4 was reported previously as a synthetic product, while compound 6 was reported as 2-hydroxy-3,6-di-sec-butylpyrazine. Herein, we report the complete NMR data for compounds 4 and 6. The compounds were evaluated for their cytotoxic activities against three cell lines. Compound 5 showed potent and selective activity against HCT-116 cell line with IC50 of 1.5 μg/mL, while 1–10 showed variable cytotoxic activities against these cancer cell lines. These results provide further understanding about the chemistry and bioactivities of the alkylated 2(1H-pyrazinone derivatives.

  14. Novel cobalt releasing sol-gel derived bioactive glass for bone tissue engineering

    International Nuclear Information System (INIS)

    Oliveira, Ana Celeste Ximenes; Barrioni, Breno Rocha; Leite, Maria de Fatima; Pereira, Marivalda Magalhaes

    2016-01-01

    Full text: Bone defects are caused by traumas, congenital disorders or infections, and bone grafts are the usual treatment. However, limitations of this therapy have lead to the advance of tissue engineering approaches. Bioactive glasses (BG) are an attractive bioactive ceramic for bone repair [1], due to its osteogenic properties and capability of releasing different ions, inducing specific biological responses. Tissue repair depends also on blood vessels formation. Among angiogenic agents, cobalt ion has been regarded as strategic component to incorporate into ion releasing materials. In this study, 5% (molar) cobalt releasing BG was synthesized by sol-gel method. To characterize the material, powder samples were evaluated by FTIR and DRX. To access the cytotoxic effects, MTT and LIVE/DEAD tests were performed on osteoblasts exposed to the ionic product of the material (100 μg/mL) for 72h. FTIR analysis reveals typical absorption bands of present groups in BG. X-ray diffractogram of DRX confirmed the amorphous character of BG, without the occurrence of recrystallization of cobalt precursor, suggesting that cobalt incorporation was well succeeded. MTT test showed that cells exposed to ionic product presented high levels of metabolic activity. LIVE/DEAD assay evidenced that cell membrane integrity and intracellular esterases activity were preserved. Both cytotoxic tests proved that cobalt-BG material generated a cell friendly environment. This work shows that BG with cobalt agent presented proper structural features and a non-cytotoxic behaviour. Reference: [1] Hench LL, J Mater Sci Mater Med 17(11), 967-78 (2006). (author)

  15. Energetics and dynamics of the non-natural fluorescent 4AP:DAP base pair

    KAUST Repository

    Chawla, Mohit; Autiero, Ida; Oliva, Romina; Cavallo, Luigi

    2018-01-01

    the experimental studies and rationalize the impact of the above non-natural bases on the structure, stability and dynamics of nucleic acid structures, we performed quantum mechanics (QM) calculations along with classical molecular dynamics (MD) simulations. QM

  16. Developments in drug delivery of bioactive alkaloids derived from traditional Chinese medicine.

    Science.gov (United States)

    Zheng, Xiao; Wu, Fei; Lin, Xiao; Shen, Lan; Feng, Yi

    2018-11-01

    The bioactive alkaloids (e.g. vincristine, hydroxycamptothecin, ligustrazine, and so on) from traditional Chinese medicine (TCM) have exerted potent efficacies (e.g. anti-tumor, anti-inflammation, immunosuppression, etc.). However, a series of undesirable physicochemical properties (like low solubility and weak stability) and baneful pharmacokinetic (PK) profiles (e.g. low bioavailability, short half time, rapid clearance, etc.) have severely restricted their applications in clinic. In addition, some side effects (like cumulative toxicities caused by high-frequency administration and their own toxicities) have recently been reported and also confined their clinical uses. Therefore, developments in drug delivery of such alkaloids are of significance in improving their drug-like properties and, thus, treatment efficiencies in clinic. Strategies, including (i) specific delivery via liposomes; (ii) sustained delivery via nanoparticles, gels, and emulsions; and (iii) transdermal delivery via ethosomes, solid lipid nanoparticles, and penetrating enhancers, have been reported to improve the pharmacokinetic and physicochemical characters of problematic TCM alkaloids, decline their adverse effects, and thus, boost their curative efficacies. In this review, the recent reports in this field were comprehensively summarized with the aim of providing an informative reference for relevant readers.

  17. Peptide mimic for influenza vaccination using nonnatural combinatorial chemistry

    Science.gov (United States)

    Miles, John J.; Tan, Mai Ping; Dolton, Garry; Galloway, Sarah A.E.; Laugel, Bruno; Makinde, Julia; Matthews, Katherine K.; Watkins, Thomas S.; Wong, Yide; Clark, Richard J.; Pentier, Johanne M.; Attaf, Meriem; Lissina, Anya; Ager, Ann; Gallimore, Awen; Gras, Stephanie; Rossjohn, Jamie; Burrows, Scott R.; Cole, David K.; Price, David A.

    2018-01-01

    Polypeptide vaccines effectively activate human T cells but suffer from poor biological stability, which confines both transport logistics and in vivo therapeutic activity. Synthetic biology has the potential to address these limitations through the generation of highly stable antigenic “mimics” using subunits that do not exist in the natural world. We developed a platform based on D–amino acid combinatorial chemistry and used this platform to reverse engineer a fully artificial CD8+ T cell agonist that mirrored the immunogenicity profile of a native epitope blueprint from influenza virus. This nonnatural peptide was highly stable in human serum and gastric acid, reflecting an intrinsic resistance to physical and enzymatic degradation. In vitro, the synthetic agonist stimulated and expanded an archetypal repertoire of polyfunctional human influenza virus–specific CD8+ T cells. In vivo, specific responses were elicited in naive humanized mice by subcutaneous vaccination, conferring protection from subsequent lethal influenza challenge. Moreover, the synthetic agonist was immunogenic after oral administration. This proof-of-concept study highlights the power of synthetic biology to expand the horizons of vaccine design and therapeutic delivery. PMID:29528337

  18. Yes to Realism! No to Non-naturalism!

    Directory of Open Access Journals (Sweden)

    Ulysses T. Araña

    2009-06-01

    Full Text Available According to contemporary moral realism a moral property, like goodness or badness, is either a natural (descriptive property or a non-natural (nondescriptive property of actions or situations. Contemporary moral naturalists like Richard Boyd, Nicholas Sturgeon, and David Brink are a group of philosophers who are often referred to as Cornell realists because of their connection with Cornell University. Frank Jackson is another contemporary moral naturalist who is one of the leaders of The Canberra Planners at the Australian National University with which he is connected. Jackson defends “the most extreme form of naturalism.” Jackson’s view is considered extremeby those who disagree with him because he believes that moral properties are reducible or identical to natural properties. This view of Jackson is opposed by contemporary non-naturalists like Jonathan Dancy, Derek Parfit, and Russ Shafer-Landau for reasons which in my view are not successful. Despite Jackson’s reductionism about the ethical, the Cornell realists, nevertheless, agree with him that moral properties are natural properties.

  19. Bioactive Secondary Metabolites from a Thai Collection of Soil and Marine-Derived Fungi of the Genera Neosartorya and Aspergillus.

    Science.gov (United States)

    Zin, War War May; Prompanya, Chadaporn; Buttachon, Suradet; Kijjoa, Anake

    2016-01-01

    Fungi are microorganisms which can produce interesting secondary metabolites with structural diversity. Although terrestrial fungi have been extensively investigated for their bioactive secondary metabolites such as antibiotics, marine-derived fungi have only recently attracted attention of Natural Products chemists. Our group has been working on the secondary metabolites produced by the cultures of the fungi of the genera Neosartorya and Aspergillus, collected from soil and marine environments from the tropical region for the purpose of finding new leads for anticancer and antibacterial drugs. This review covers only the secondary metabolites of four soil and six marine-derived species of Neosarorya as well as a new species of marine-derived Aspergillus, investigated by our group. In total, we have isolated fifty three secondary metabolites which can be categorized as polyketides (two), isocoumarins (six), terpenoids (two), meroterpenes (fourteen), alkaloids (twenty eight) and cyclic peptide (one). The anticancer and antibacterial activities of these fungal metabolites are also discussed. Among fifty three secondary metabolites isolated, only the alkaloid eurochevalierine and the cadinene sesquiterpene, isolated from the soil fungus N. pseudofisheri, showed relevant in vitro cytostatic activity against glioblastoma (U373) and non-small cell lung cancer (A549) cell lines while the meroditerpene aszonapyrone A exhibited strong antibacterial activity against multidrug-resistant Gram-positive bacteria and also strong antibiofilm activity in these isolates.

  20. Structure, Content, and Bioactivity of Food-Derived Peptides in the Body.

    Science.gov (United States)

    Sato, Kenji

    2018-03-28

    Orally administered peptides are assumed to be degraded into amino acids in the body. However, our recent studies revealed some food-derived prolyl and pyroglutamyl peptides with 2-3 amino acid residues in the blood of humans and animals, while most of the peptides in the endoproteinase digest of food protein are degraded by exopeptidase. Some food-derived dipeptides in the body display in vitro and in vivo biological activities. These facts indicate that the biological activities of food-derived peptides in the body rather than those in food are crucial to understanding the mechanism of the beneficial effects of orally administered peptides.

  1. Bioactive Pentacyclic Triterpene Ester Derivatives from Alnus viridis ssp. viridis Bark.

    Science.gov (United States)

    Novakovic, Miroslav; Nikodinovic-Runic, Jasmina; Veselinovic, Jovana; Ilic-Tomic, Tatjana; Vidakovic, Vera; Tesevic, Vele; Milosavljevic, Slobodan

    2017-05-26

    Seven derivatives of pentacyclic triterpene acids (1-7) were isolated from the bark of Alnus viridis ssp. viridis using a combination of column chromatography and semipreparative HPLC. Compounds 1-3, 6, and 7 were determined to be new after spectroscopic data interpretation and were assigned as 27-hydroxyalphitolic acid derivatives (1-3), a 27-hydroxybetulinic acid derivative (6), and a 3-epi-maslinic acid derivative (7), respectively. Pentacyclic triterpenoids with a C-27 hydroxymethyl group have been found in species of the genus Alnus for the first time. These compounds were subjected to cytotoxicity testing against a number of cancer cell lines. Also, selected pentacyclic triterpenoids were selected as potential inhibitors of topoisomerases I and IIα for an in silico investigation.

  2. Role of SrO on the bioactivity behavior of some ternary borate glasses and their glass ceramic derivatives

    Science.gov (United States)

    Abdelghany, A. M.; Ouis, M. A.; Azooz, M. A.; ElBatal, H. A.; El-Bassyouni, G. T.

    2016-01-01

    Borate glasses containing SrO substituting both CaO and NaO were prepared and characterized for their bioactivity or bone bonding ability. Glass ceramic derivatives were prepared by thermal heat treatment process. FTIR, XRD and SEM measurements for the prepared glass and glass-ceramics before and after immersion in sodium phosphate solution for one and two weeks were carried out. The appearance of two IR peaks within the range 550-680 cm-1 after immersion in phosphate solution indicates the formation of hydroxyapatite or equivalent Sr phosphate layer. X-ray diffraction data agree with the FTIR spectral analysis. The solubility test was carried out for both glasses and glass ceramics derivatives in the same phosphate solution. The introduction of SrO increases the solubility for both glasses and glass ceramics and this is assumed to be due to the formation of Sr phosphate which is more soluble than calcium phosphate (hydroxyapatite). SEM images reveal varying changes in the surfaces of glass ceramics after immersion according to the SrO content.

  3. Role of SrO on the bioactivity behavior of some ternary borate glasses and their glass ceramic derivatives.

    Science.gov (United States)

    Abdelghany, A M; Ouis, M A; Azooz, M A; ElBatal, H A; El-Bassyouni, G T

    2016-01-05

    Borate glasses containing SrO substituting both CaO and NaO were prepared and characterized for their bioactivity or bone bonding ability. Glass ceramic derivatives were prepared by thermal heat treatment process. FTIR, XRD and SEM measurements for the prepared glass and glass-ceramics before and after immersion in sodium phosphate solution for one and two weeks were carried out. The appearance of two IR peaks within the range 550-680cm(-1) after immersion in phosphate solution indicates the formation of hydroxyapatite or equivalent Sr phosphate layer. X-ray diffraction data agree with the FTIR spectral analysis. The solubility test was carried out for both glasses and glass ceramics derivatives in the same phosphate solution. The introduction of SrO increases the solubility for both glasses and glass ceramics and this is assumed to be due to the formation of Sr phosphate which is more soluble than calcium phosphate (hydroxyapatite). SEM images reveal varying changes in the surfaces of glass ceramics after immersion according to the SrO content. Copyright © 2015 Elsevier B.V. All rights reserved.

  4. Genotype-driven isolation of enterocin with novel bioactivities from mangrove-derived Streptomyces qinglanensis 172205.

    Science.gov (United States)

    Xu, Dong-Bo; Ma, Min; Deng, Zi-Xin; Hong, Kui

    2015-07-01

    The type II polyketide synthase (PKS) natural product enterocin (1) was isolated from a mangrove-derived novel species Streptomyces qinglanensis 172205 guided by genome sequence, and its putative biosynthetic gene cluster was revealed. Its natural analogues 5-deoxyenterocin (2) and wailupemycin A-C (3-5) were also identified by tandem mass spectrometry. By feeding experiments with aryl acids, strain 172205 was proved to incorporate partial exogenous starter units into enterocin- and wailupemycin-based analogues, thus being a new and suitable microorganism for engineering unnatural enc-derived polyketide metabolites. In addition, biological assays indicated that enterocin showed obvious inhibitory activity against β-amyloid protein (Aβ1-42) fibrillation and moderate cytotoxicity against HeLa and HepG2 for the first time.

  5. Bioactive Indole Derivatives from the South Pacific Marine Sponges Rhopaloeides odorabile and Hyrtios sp.

    Directory of Open Access Journals (Sweden)

    Marie-Lise Bourguet-Kondracki

    2011-05-01

    Full Text Available Indole derivatives including bromoindoles have been isolated from the South Pacific marine sponges Rhopaloeides odorabile and Hyrtios sp. Their structures were established through analysis of mass spectra and 1D and 2D NMR spectroscopic data. Their potential inhibitory phospholipase A2 (PLA2, antioxidant and cytotoxic activities were evaluated. The new derivative 5,6-dibromo-l-hypaphorine (9 isolated from Hyrtios sp. revealed a weak bee venom PLA2 inhibition (IC50 0.2 mM and a significant antioxidant activity with an Oxygen Radical Absorbance Capacity (ORAC value of 0.22. The sesquiterpene aureol (4, also isolated from Hyrtios sp., showed the most potent antioxidant activity with an ORAC value of 0.29.

  6. Synthesis of novel bioactive lactose-derived oligosaccharides by microbial glycoside hydrolases

    Science.gov (United States)

    Díez-Municio, Marina; Herrero, Miguel; Olano, Agustín; Moreno, F Javier

    2014-01-01

    Prebiotic oligosaccharides are increasingly demanded within the Food Science domain because of the interesting healthy properties that these compounds may induce to the organism, thanks to their beneficial intestinal microbiota growth promotion ability. In this regard, the development of new efficient, convenient and affordable methods to obtain this class of compounds might expand even further their use as functional ingredients. This review presents an overview on the most recent interesting approaches to synthesize lactose-derived oligosaccharides with potential prebiotic activity paying special focus on the microbial glycoside hydrolases that can be effectively employed to obtain these prebiotic compounds. The most notable advantages of using lactose-derived carbohydrates such as lactosucrose, galactooligosaccharides from lactulose, lactulosucrose and 2-α-glucosyl-lactose are also described and commented. PMID:24690139

  7. A bioactive molecule in a complex wound healing process: platelet-derived growth factor.

    Science.gov (United States)

    Kaltalioglu, Kaan; Coskun-Cevher, Sule

    2015-08-01

    Wound healing is considered to be particularly important after surgical procedures, and the most important wounds related to surgical procedures are incisional, excisional, and punch wounds. Research is ongoing to identify methods to heal non-closed wounds or to accelerate wound healing; however, wound healing is a complex process that includes many biological and physiological events, and it is affected by various local and systemic factors, including diabetes mellitus, infection, ischemia, and aging. Different cell types (such as platelets, macrophages, and neutrophils) release growth factors during the healing process, and platelet-derived growth factor is a particularly important mediator in most stages of wound healing. This review explores the relationship between platelet-derived growth factor and wound healing. © 2014 The International Society of Dermatology.

  8. Marine Sponge Derived Natural Products between 2001 and 2010: Trends and Opportunities for Discovery of Bioactives

    Science.gov (United States)

    Mehbub, Mohammad Ferdous; Lei, Jie; Franco, Christopher; Zhang, Wei

    2014-01-01

    Marine sponges belonging to the phylum Porifera (Metazoa), evolutionarily the oldest animals are the single best source of marine natural products. The present review presents a comprehensive overview of the source, taxonomy, country of origin or geographical position, chemical class, and biological activity of sponge-derived new natural products discovered between 2001 and 2010. The data has been analyzed with a view to gaining an outlook on the future trends and opportunities in the search for new compounds and their sources from marine sponges. PMID:25196730

  9. Synthesis, Antiviral Bioactivity of Novel 4-Thioquinazoline Derivatives Containing Chalcone Moiety

    Directory of Open Access Journals (Sweden)

    Zhihua Wan

    2015-06-01

    Full Text Available A series of novel 4-thioquinazoline derivatives containing chalcone moiety were designed, synthesized and systematically evaluated for their antiviral activity against TMV. The bioassay results showed that most of these compounds exhibited moderate to good anti-TMV activity. In particular, compounds M2 and M6 possessed appreciable protection activities against TMV in vivo, with 50% effective concentration (EC50 values of 138.1 and 154.8 μg/mL, respectively, which were superior to that of Ribavirin (436.0 μg/mL. The results indicated that chalcone derivatives containing 4-thioquinazoline moiety could effectively control TMV. Meanwhile, the structure-activity relationship (SAR of the target compounds, studied using the three-dimensional quantitative structure-activity relationship (3D-QSAR method of comparative molecular field analysis (CoMFA based on the protection activities against TMV, demonstrated that the CoMFA model exhibited good predictive ability with the cross-validated q2 and non-cross-validated r2 values of 0.674 and 0.993, respectively. Meanwhile, the microscale thermophoresis (MST experimental showed that the compound M6 may interaction with the tobacco mosaic virus coat protein (TMV CP.

  10. Identification of gut-derived metabolites of maslinic acid, a bioactive compound from Olea europaea L.

    Science.gov (United States)

    Lozano-Mena, Glòria; Sánchez-González, Marta; Parra, Andrés; Juan, M Emília; Planas, Joana M

    2016-09-01

    Maslinic acid has been described to exert a chemopreventive activity in colon cancer. Hereby, we determined maslinic acid and its metabolites in the rat intestine previous oral administration as a first step in elucidating whether this triterpene might be used as a nutraceutical. Maslinic acid was orally administered at 1, 2, and 5 mg/kg to male Sprague-Dawley for 2 days. At 24 h after the last administration, the content of the duodenum and jejunum, ileum, cecum, and colon was collected and extracted with methanol 80% prior to LC-APCI-MS analysis. The developed method was validated providing suitable sensitivity (LOQ of 5 nM), good recovery (97.8 ± 3.6%), linear correlation, and appropriate precision (< 9%). Maslinic acid was detected in all the segments with higher concentrations in the distal part of the intestine. LC-APCI-LTQ-ORBITRAP-MS allowed the identification of 11 gut-derived metabolites that were formed by mono-, dihydroxylation, and dehydrogenation reactions. Maslinic acid undergoes phase I reactions resulting in a majority of monohydroxylated metabolites without the presence of phase II derivatives. The high concentration of maslinic acid achieved in the intestine suggests that it could exert a beneficial effect in the prevention of colon cancer. © 2016 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

  11. A New Acetylenic Compound and Other Bioactive Metabolites from a Shark Gill-derived Penicillium Strain

    Directory of Open Access Journals (Sweden)

    Yi Zhang

    2017-01-01

    Full Text Available Nine chiral compounds (1−9 were isolated from the static fermentation culture of a shark gill-derived fungus Penicillium polonicum AP2T1. These compounds include a new acetylenic aromatic ether (1 , (--WA , four alkaloids ( a urantiomide C ( 2 , fructigenine A (3, cyclopenin (4 and cyclopenol (5 and four oxygenated compounds ((R-penipratynolene (6, (3S,4S-3,4-dihydro-3,4,8-trihydroxyl-naphthalenone (7, verrucosidin (8 and norverrucosidin (9. Their structures were elucidated by MS, NMR , optical rotation and circular dichroism (CD . In antimicrobial tests , compounds 1–4, 6 and 8–9 showed weak antibacterial activity against Staphylococcus aureus, Bacillus subtilis, and/or Escherichia coli.Compounds 3, 8 and 9 also exhibited moderate toxicity against Artemia salina larva , and showed cytotoxicity against human colon cancer cell line HCT116.

  12. Synthesis and Bioactivities of Novel Pyrazole Oxime Derivatives Containing a 5-Trifluoromethylpyridyl Moiety

    Directory of Open Access Journals (Sweden)

    Hong Dai

    2016-02-01

    Full Text Available In this study, in order to find novel biologically active pyrazole oxime compounds, a series of pyrazole oxime derivatives containing a 5-trifluoromethylpyridyl moiety were synthesized. Preliminary bioassays indicated that most title compounds were found to display good to excellent acaricidal activity against Tetranychus cinnabarinus at a concentration of 200 μg/mL, and some designed compounds still showed excellent acaricidal activity against Tetranychus cinnabarinus at the concentration of 10 μg/mL, especially since the inhibition rates of compounds 8e, 8f, 8l, 8m, 8n, 8p, and 8q were all 100.00%. Interestingly, some target compounds exhibited moderate to good insecticidal activities against Plutella xylostella and Aphis craccivora at a concentration of 200 μg/mL; furthermore, compounds 8e and 8l possessed outstanding insecticidal activities against Plutella xylostella under the concentration of 50 μg/mL.

  13. Hydroquinone; A novel bioactive compound from plant-derived smoke can cue seed germination of lettuce

    Science.gov (United States)

    Kamran, Muhammad; Khan, Abdul L.; Ali, Liaqat; Hussain, Javid; Waqas, Muhammad; Al-Harrasi, Ahmed; Imran, Qari M.; Kim, Yoon-Ha; Kang, Sang-Mo; Yun, Byung-Wook; Lee, In-Jung

    2017-05-01

    Plant-derived smoke has been known to play an important role in distribution and growth of vegetation. Using a proficiently designed furnace, we extracted smoke from the leaves of four plant viz. Helianthus annuus, Aloe vera, Ginkgo biloba, and Cymbopogon jwarancusa. Smoke dilutions obtained from these plants were obtained in different concentrations to identify potential lettuce growth promoting smoke solution. Results revealed that smoke obtained from Ginkgo biloba significantly enhanced the lettuce seed germination. This solution was then partitioned into ethyl acetate, dichloromethane, n-hexane, chloroform and ether fractions. Ethyl acetate fraction was found to be potent to enhance seed germination. This fraction was subjected to column chromatography and spectroscopic techniques to obtain compound 1. This compound was identified as hydroquinone using 1D and 2D NMR techniques. At low concentrations (5, 10 and 20 ppm), compound 1 enhanced the lettuce seed germination; however, higher concentrations inhibited its growth as compared to control.

  14. Hydroquinone; A Novel Bioactive Compound from Plant-Derived Smoke Can Cue Seed Germination of Lettuce

    Science.gov (United States)

    Kamran, Muhammad; Khan, Abdul L.; Ali, Liaqat; Hussain, Javid; Waqas, Muhammad; Al-Harrasi, Ahmed; Imran, Qari M.; Kim, Yoon-Ha; Kang, Sang-Mo; Yun, Byung-Wook; Lee, In-Jung

    2017-01-01

    Plant-derived smoke has been known to play an important role in distribution and growth of vegetation. Using a proficiently designed furnace, we extracted smoke from the leaves of four plant viz. Helianthus annuus,Aloe vera,Ginkgo biloba, and Cymbopogon jwarancusa. Smoke dilutions obtained from these plants were obtained in different concentrations to identify potential lettuce growth promoting smoke solution. Results revealed that smoke obtained from G. biloba significantly enhanced the lettuce seed germination. This solution was then partitioned into ethyl acetate, dichloromethane, n-hexane, chloroform and ether fractions. Ethyl acetate fraction was found to be potent to enhance seed germination. This fraction was subjected to column chromatography and spectroscopic techniques to obtain compound 1. This compound was identified as hydroquinone using 1D and 2D NMR techniques. At low concentrations (5, 10, and 20 ppm), compound 1 enhanced the lettuce seed germination; however, higher concentrations inhibited its growth as compared to control. PMID:28553632

  15. Synthesis and Bioactivity of N-Benzoyl-N'-[5-(2'-substituted phenyl-2-furoyl] Semicarbazide Derivatives

    Directory of Open Access Journals (Sweden)

    Zining Cui

    2010-06-01

    Full Text Available In order to find novel chitin synthesis inhibitors (CSIs with good activity, benzoylphenylurea, a typical kind of CSIs, was chosen as the lead compound and 15 novel derivatives containing furan moieties were designed by converting the urea linkage of benzoylphenylureas into a semicarbazide and changing the aniline part into furoyl groups. The title compounds were synthesized by the reaction of substituted benzoyl isocyanates with 5-(substituted phenyl-2-furoyl hydrazine, and the structures were confirmed by IR, 1H-NMR, elemental analysis and single crystal X-ray diffraction analyses (compound E2. The bioassay results indicated that the title compounds exhibit good insecticidal activity, especially towards Plutella xylostella L., but had lower fungicidal activity. Inspiringly, the title compounds possessed obvious anticancer activity against human promyelocytic leukemic cell line (HL-60, and some of the title compounds also had activity against human hepatocellular carcinoma cell line (Bel-7402, human gastric carcinoma cell line (BGC-823, and human nasopharyngeal carcinoma cell line (KB. The results indicated that the linkage in the lead compounds was important to the bioactivity and spectra. The modification on the urea linkage is an effective strategy to discover new pesticide and drug candidates.

  16. Immobilization-stabilization of proteins on nanofibrillated cellulose derivatives and their bioactive film formation.

    Science.gov (United States)

    Arola, Suvi; Tammelin, Tekla; Setälä, Harri; Tullila, Antti; Linder, Markus B

    2012-03-12

    In a number of different applications for enzymes and specific binding proteins a key technology is the immobilization of these proteins to different types of supports. In this work we describe a concept for protein immobilization that is based on nanofibrillated cellulose (NFC). NFC is a form of cellulose where fibers have been disintegrated into fibrils that are only a few nanometers in diameter and have a very large aspect ratio. Proteins were conjugated through three different strategies using amine, epoxy, and carboxylic acid functionalized NFC. The conjugation chemistries were chosen according to the reactive groups on the NFC derivatives; epoxy amination, heterobifunctional modification of amino groups, and EDC/s-NHS activation of carboxylic acid groups. The conjugation reactions were performed in solution and immobilization was performed by spin coating the protein-NCF conjugates. The structure of NFC was shown to be advantageous for both protein performance and stability. The use of NFC allows all covalent chemistry to be performed in solution, while the immobilization is achieved by a simple spin coating or spreading of the protein-NFC conjugates on a support. This allows more scalable methods and better control of conditions compared to the traditional methods that depend on surface reactions.

  17. Bioactivity of Turmeric-Derived Curcuminoids and Related Metabolites in Breast Cancer

    Science.gov (United States)

    Wright, Laura E.; Frye, Jen B.; Gorti, Bhavana; Timmermann, Barbara N.; Funk, Janet L.

    2013-01-01

    While the chemotherapeutic effect of curcumin, one of three major curcuminoids derived from turmeric, has been reported, largely unexplored are the effects of complex turmeric extracts more analogous to traditional medicinal preparations, as well as the relative importance of the three curcuminoids and their metabolites as anti-cancer agents. These studies document the pharmacodynamic effects of chemically-complex turmeric extracts relative to curcuminoids on human breast cancer cell growth and tumor cell secretion of parathyroid hormone-related protein (PTHrP), an important driver of cancer bone metastasis. Finally, relative effects of structurally-related metabolites of curcuminoids were assessed on the same endpoints. We report that 3 curcuminoid-containing turmeric extracts differing with respect to the inclusion of additional naturally occurring chemicals (essential oils and/or polar compounds) were equipotent in inhibiting human breast cancer MDA-MB-231 cell growth (IC50=10–16μg/mL) and secretion of osteolytic PTHrP (IC50=2–3μg/mL) when concentrations were normalized to curcuminoid content. Moreover, these effects were curcuminoid-specific, as botanically-related gingerol containing extracts had no effect. While curcumin and bis-demethoxycurcumin were equipotent to each other and to the naturally occurring curcuminoid mixture (IC50=58 μM), demethoxycurcumin was without effect on cell growth. However, each of the individual curcuminoids inhibited PTHrP secretion (IC50=22–31μM) to the same degree as the curcuminoid mixture (IC50=16 μM). Degradative curcuminoid metabolites (vanillin and ferulic acid) did not inhibit cell growth or PTHrP, while reduced metabolites (tetrahydrocurcuminoids) had inhibitory effects on cell growth and PTHrP secretion but only at concentrations ≥10-fold higher than the curcuminoids. These studies emphasize the structural and biological importance of curcuminoids in the anti-breast cancer effects of turmeric and contradict

  18. Topology and parameter data of thirteen non-natural amino acids for molecular simulations with CHARMM22

    Directory of Open Access Journals (Sweden)

    Olujide O. Olubiyi

    2016-12-01

    Full Text Available In this article we provide a data package containing the topology files and parameters compatible with the CHARMM22 force field for thirteen non-natural amino acids. The force field parameters were derived based on quantum mechanical (QM calculations involving geometry optimization and potential energy surface scanning at the HF 6-31G(d and HF 6-311G(d,p levels of theory. The resulting energy data points were fitted to mathematical functions representing each component of the CHARMM22 force field. Further fine-tuning of the parameters utilized molecular mechanics energies, which were iteratively calculated and compared to the corresponding QM values until the latter were satisfactorily reproduced. The final force field data were validated with molecular dynamics simulations in explicit solvent conditions.

  19. Bioactive lipid coating of bone allografts directs engraftment and fate determination of bone marrow-derived cells in rat GFP chimeras

    OpenAIRE

    Das, Anusuya; Segar, Claire E.; Chu, Yihsuan; Wang, Tiffany W.; Lin, Yong; Yang, Chunxi; Du, Xeujun; Ogle, Roy C.; Cui, Quanjun; Botchwey, Edward A.

    2015-01-01

    Bone grafting procedures are performed to treat wounds incurred during wartime trauma, accidents, and tumor resections. Endogenous mechanisms of repair are often insufficient to ensure integration between host and donor bone and subsequent restoration of function. We investigated the role that bone marrow-derived cells play in bone regeneration and sought to increase their contributions by functionalizing bone allografts with bioactive lipid coatings. Polymer-coated allografts were used to lo...

  20. Development of a composite based on hydroxyapatite and magnesium and zinc‐containing sol–gel-derived bioactive glass for bone substitute applications

    International Nuclear Information System (INIS)

    Ashuri, Maziar; Moztarzadeh, Fathollah; Nezafati, Nader; Ansari Hamedani, Ali; Tahriri, Mohammadreza

    2012-01-01

    In the present study, a bioceramic-based composite was prepared by sintering compacts made up of mixtures of hydroxyapatite (HA) and sol–gel-derived bioactive glass (64SiO 2 -26CaO-5MgO-5ZnO) (based on mol%) powders. HA powder was mixed with different concentrations of the glass powders up to 30 wt.%. The effect of adding bioactive glass powder to HA matrix, on the mechanical properties of the composite was assessed by compression test. The specimen with the highest compressive strength was chosen to be immersed in simulated body fluid (SBF) to study apatite forming ability and dissolution behavior. It was found that compressive strength of the specimen was decreased 65% after maintaining in the SBF for 14 days. X-ray diffraction (XRD) showed prevalence of HA and β-TCP related peaks. Also, the surface morphology of the composite was observed using scanning electron microscopy (SEM). The study of degradation behavior revealed Si release capability of this composite. Biological evaluations in vitro confirmed the composite studied could induce osteoblast-like cells' activities. - Highlights: ► A novel composite based on HA/bioactive glass for bone substitutes was developed. ► Evaluations in vitro confirmed the composites induce bone-like cells' activities. ► A successful compromise of bioactivity and cytocompatibility was observed.

  1. A novel strategy of spine defect repair with a degradable bioactive scaffold preloaded with adipose-derived stromal cells.

    Science.gov (United States)

    Liang, Haixiang; Li, Xudong; Shimer, Adam L; Balian, Gary; Shen, Francis H

    2014-03-01

    Although the use of mesenchymal stem cells (MSC) with scaffolds for bone repair has been considered an effective method, the interactions between implanted materials and bone tissues have not been fully elucidated. At some specific sites, such as the vertebral body (VB) of the spine, the process of bone repair with implanted biomaterials is rarely reported. Recently, adipose tissue was found to be an alternative source of MSC besides bone marrow. However, the strategy of using adipose-derived stromal (ADS) cells with bioactive scaffold for the repair of spinal bone defects has seldom been studied. To use a sintered poly(lactide-co-glycolide) acid (PLGA) microspheres scaffold seeded with induced rat ADS cells to repair a bone defect of the VB in a rat model. Basic science and laboratory study. A sintered porous microspheres scaffold was manufactured by PLGA. ADS cells were isolated from Fischer 344 rats and then induced by osteogenic medium with growth and differentiation factor 5 (GDF5) in vitro. Before implantation, cells were cultured with inductive media for 2 weeks as a monolayer situation and 1 more week on a PLGA scaffold as a three-dimensional structure. These assembled bioactive scaffolds then were implanted in lumbar VB bone defects in Fischer 344 rats. The ex vivo differentiation of the cells was confirmed by von Kossa staining and real-time polymerase chain reaction. The performance of cells on the scaffold was detected by scanning electron microscopy and (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium) assay. In vivo bone formation was quantitatively measured by computed tomography study. And the effect of tissue repair was also evaluated by histological studies. Proliferation and differentiation of cells were confirmed before in vivo implantation. Quantification of bone formation in vivo through serial three-dimensional computed tomography images revealed that the VB implanted with GDF5-induced cells

  2. Properties of a non-bioactive fluorescent derivative of differentiation-inducing factor-3, an anti-tumor agent found in Dictyostelium discoideum

    Directory of Open Access Journals (Sweden)

    Yuzuru Kubohara

    2014-03-01

    Full Text Available Differentiation-inducing factor-3 (DIF-3, found in the cellular slime mold Dictyostelium discoideum, and its derivatives, such as butoxy-DIF-3 (Bu-DIF-3, are potent anti-tumor agents. To investigate the activity of DIF-like molecules in tumor cells, we recently synthesized a green fluorescent DIF-3 derivative, BODIPY-DIF-3G, and analyzed its bioactivity and cellular localization. In this study, we synthesized a red (orange fluorescent DIF-3 derivative, BODIPY-DIF-3R, and compared the cellular localization and bioactivities of the two BODIPY-DIF-3s in HeLa human cervical cancer cells. Both fluorescent compounds penetrated the extracellular membrane within 0.5 h and localized mainly to the mitochondria. In formalin-fixed cells, the two BODIPY-DIF-3s also localized to the mitochondria, indicating that the BODIPY-DIF-3s were incorporated into mitochondria independently of the mitochondrial membrane potential. After treatment for 3 days, BODIPY-DIF-3G, but not BODIPY-DIF-3R, induced mitochondrial swelling and suppressed cell proliferation. Interestingly, the swollen mitochondria were stainable with BODIPY-DIF-3G but not with BODIPY-DIF-3R. When added to isolated mitochondria in vitro, BODIPY-DIF-3G increased dose-dependently the rate of O2 consumption, but BODIPY-DIF-3R did not. These results suggest that the bioactive BODIPY-DIF-3G suppresses cell proliferation, at least in part, by altering mitochondrial activity, whereas the non-bioactive BODIPY-DIF-3R localizes to the mitochondria but does not affect mitochondrial activity or cell proliferation.

  3. Bioactive substances

    Digital Repository Service at National Institute of Oceanography (India)

    Wahidullah, S.

    Chemistry related to certain bioactive molecules, from Indian Ocean Region, developed into drugs or which served as models for the synthesis of more effective bioactive substances or in use in fundamental studies of physiological and biochemical...

  4. Effectiveness of bovine-derived xenograft versus bioactive glass with periodontally accelerated osteogenic orthodontics in adults: a randomized, controlled clinical trial.

    Science.gov (United States)

    Bahammam, Maha A

    2016-11-30

    Periodontally accelerated osteogenic orthodontics (PAOO) combines periodontal therapy with orthodontic therapy, which minimises treatment time. This study compared the effectiveness of a bovine-derived xenograft with that of bioactive glass when combined with PAOO for the treatment of adult patients with moderate crowding of the teeth. In this prospective, single-masked clinical trial, 33 orthodontic patients (20 women, 13 men; mean age 21.2 ± 1.43 [18 - 27] years), were randomly allocated to one of three groups. Group 1 underwent a modified corticotomy technique on the labial side only, whereas group 2 was treated with the same technique combined with PAOO using a bovine-derived xenograft and group 3 was treated in the same way but combining PAOO with bioactive glass. The total treatment duration was recorded from the start of active orthodontic treatment, immediately after corticotomy, and at the time of debonding. Probing depth was evaluated clinically and bone density and root length were evaluated radiographically on the day of surgery (baseline, T1), post-treatment at debonding (T2), and 9 months post-treatment (T3). The duration of orthodontic treatment was markedly reduced to an average of 11.4 ± 0.14 weeks in all groups. All probing depths were orthodontic treatment and periodontal surgery is an effective treatment for adult patients that decreases the duration of active treatment and reduces the risk of root resorption. Use of a bovine-derived xenograft with modified corticotomy provided superior benefits in terms of increased bone density than did the use of bioactive glass. The study was retrospectively registered at ClinicalTrials.gov under Clinical Trial Registration Number: NCT02796911 .

  5. Phytic acid derived bioactive CaO-P2O5-SiO2 gel-glasses.

    Science.gov (United States)

    Li, Ailing; Qiu, Dong

    2011-12-01

    The possibility of using phytic acid as a precursor to synthesize CaO-P(2)O(5)-SiO(2) glasses by sol-gel method has been explored and the pseudo ternary phase diagram has been established. It was shown that gel-glasses over a broader range of compositions could be prepared compared to other phosphorus precursors or melt-quenching method. Furthermore, phytic acid was found to assist calcium being incorporated into glass networks. In vitro tests in simulated body fluid (SBF) were performed on the above gel-glasses and it was found that they were bioactive over a much broader compositional range especially at high phosphate content, thus enabling one to design bioactive materials with various degradation rates by adjusting the phosphate content.

  6. The In Vitro Bioactivity, Degradation, and Cytotoxicity of Polymer-Derived Wollastonite-Diopside Glass-Ceramics

    Directory of Open Access Journals (Sweden)

    Amanda De Castro Juraski

    2017-04-01

    Full Text Available Ca-Mg silicates are receiving a growing interest in the field of bioceramics. In a previous study, wollastonite-diopside (WD glass-ceramics were successfully prepared by a new processing route, consisting of the heat treatment of a silicone resin embedding reactive oxide particles and a Ca/Mg-rich glass. The in vitro degradation, bioactivity, and cell response of these new WD glass-ceramics, fired at 900–1100 °C for 1 h, as a function of the Ca/Mg-rich glass content, are the aim of this investigation The results showed that WD glass-ceramics from formulations comprising different glass contents (70–100% at 900 °C, 30% at 1100 °C exhibit the formation of an apatite-like layer on their surface after immersion in SBF for seven days, thus confirming their surface bioactivity. The XRD results showed that these samples crystallized, mainly forming wollastonite (CaSiO3 and diopside (CaMgSi2O6, but combeite (Na2Ca2Si3O9 crystalline phase was also detected. Besides in vitro bioactivity, cytotoxicity and osteoblast adhesion and proliferation tests were applied after all characterizations, and the formulation comprising 70% glass was demonstrated to be promising for further in vivo studies.

  7. Combined genetic and bioactivity-based prioritization leads to the isolation of an endophyte-derived antimycobacterial compound.

    Science.gov (United States)

    Alvin, A; Kalaitzis, J A; Sasia, B; Neilan, B A

    2016-05-01

    To initiate a genetic and bioactivity-based screening programme of culturable endophytes to identify micro-organisms capable of producing bioactive polyketides and peptides. Fungal endophytes were isolated from flowers, leaves and roots of Rhoeo spathacea, revealing a community consisting of Colletotrichum sp., Fusarium sp., Guignardia sp., Phomopsis sp., Phoma sp. and Microdochium sp. Genetic screening showed that all isolates had polyketide synthase (PKS) genes and most had nonribosomal peptide synthetase (NRPS) genes. Ethyl acetate extracts of the fungal isolates exhibited antiproliferative activity against at least one of the seven bacterial and mycobacterial test strains. Nuclear Magnetic Resonance -guided fractionation of the crude extract from a Fusarium sp. strain which exhibited strong antiproliferative activity against Mycobacterium tuberculosis resulted in the isolation of the polyketide javanicin. This compound was active against Myco. tuberculosis (MIC = 25 μg ml(-1)) and Mycobacterium phlei (MIC = 50 μg ml(-1)). The medicinal plant R. spathacea hosts a variety of fungal endophytes capable of producing antibacterial and antimycobacterial compounds. There is a positive correlation between the presence of PKS and/or NRPS encoding genes in endophytes and the bioactivity of their respective organic extracts. This is the first report on the fungal endophytic diversity of R. spathacea, and the isolation of an antimycobacterial compound from the plant which has been traditionally used for the treatment of tuberculosis symptoms. © 2016 The Society for Applied Microbiology.

  8. The In Vitro Bioactivity, Degradation, and Cytotoxicity of Polymer-Derived Wollastonite-Diopside Glass-Ceramics

    Science.gov (United States)

    Juraski, Amanda De Castro; Dorion Rodas, Andrea Cecilia; Elsayed, Hamada; Bernardo, Enrico; Oliveira Soares, Viviane; Daguano, Juliana

    2017-01-01

    Ca-Mg silicates are receiving a growing interest in the field of bioceramics. In a previous study, wollastonite-diopside (WD) glass-ceramics were successfully prepared by a new processing route, consisting of the heat treatment of a silicone resin embedding reactive oxide particles and a Ca/Mg-rich glass. The in vitro degradation, bioactivity, and cell response of these new WD glass-ceramics, fired at 900–1100 °C for 1 h, as a function of the Ca/Mg-rich glass content, are the aim of this investigation The results showed that WD glass-ceramics from formulations comprising different glass contents (70–100% at 900 °C, 30% at 1100 °C) exhibit the formation of an apatite-like layer on their surface after immersion in SBF for seven days, thus confirming their surface bioactivity. The XRD results showed that these samples crystallized, mainly forming wollastonite (CaSiO3) and diopside (CaMgSi2O6), but combeite (Na2Ca2Si3O9) crystalline phase was also detected. Besides in vitro bioactivity, cytotoxicity and osteoblast adhesion and proliferation tests were applied after all characterizations, and the formulation comprising 70% glass was demonstrated to be promising for further in vivo studies. PMID:28772783

  9. New generation poly(ε-caprolactone)/gel-derived bioactive glass composites for bone tissue engineering: Part I. Material properties.

    Science.gov (United States)

    Dziadek, Michal; Menaszek, Elzbieta; Zagrajczuk, Barbara; Pawlik, Justyna; Cholewa-Kowalska, Katarzyna

    2015-11-01

    Poly(ε-caprolactone) (PCL) based composite films containing 12 and 21vol.% bioactive glass (SBG) microparticles were prepared by solvent casting method. Two gel-derived SBGs of SiO2-CaO-P2O5 system differing in SiO2 and CaO contents were applied (mol%): S2: 80SiO2, 16CaO, 4P2O5 and A2: 40SiO2, 54CaO, 6P2O5. The surfaces of the films in contact with Petri dish and exposed to the gas phase during casting were denoted as GS and AS, respectively. Both surfaces of films were characterised in terms of their morphology, micro- and nano-topography as well as wettability. Also mechanical properties (tensile strength, Young's modulus) and PCL matrix crystallinity (degree of crystallinity, crystal size) were evaluated. Degradation behaviour was examined by incubation of materials in UHQ-water at 37°C for 56weeks. The crystallinity, melting temperature and mass loss of incubated materials and pH changes of water were monitored. Furthermore, proliferation of MG-63 osteoblastic cells by direct contact and cytotoxic effect of obtained materials were investigated. Results showed that opposite surfaces of the same polymer and composite films differ in studied surface parameters. The addition of SBG particles into PCL matrix improves nano- and micro-roughness of both surfaces, enhances the hydrophilicity of GS surfaces (~67° for 21A2-PCL compared to ~78° for pure PCL) and also makes AS surface more hydrophobic (~94° for 21S2-PCL compared to ~86° for pure PCL). The nucleation density of PCL was increased with increasing content of SBG particles, which results in the large number of fine spherulites on composite AS surfaces observed using polarized optical (POM), scanning electron (SEM), and atomic force (AFM) microscopies. Higher content of SBG particles causes a notable increase of Young's modulus (from 0.38GPa for pure PCL, 0.90GPa for 12A2-PCL to 1.31GPa for 21A2-PCL), which also depends on SBG chemical composition. After 56-week degradation test, considerably higher

  10. Evaluation of snake venom phospholipase A{sub 2}: hydrolysis of non-natural esters

    Energy Technology Data Exchange (ETDEWEB)

    Pirolla, Renan A.S.; Baldasso, Paulo A.; Marangoni, Sergio; Moran, Paulo J.S.; Rodrigues, Jose Augusto R., E-mail: jaugusto@iqm.unicamp.b [University of Campinas (UNICAMP), SP (Brazil). Inst. of Chemistry. Dept. of Organic Chemistry

    2011-07-01

    Phospholipase A2 from the rattlesnake Crotalus durissus terrificus was employed for the first time to test its enantioselectivity on the hydrolysis of different non-natural esters. It was observed that the structure of this small enzyme is restrictive in the choice of its lipase action with non-natural substrates. Two forms of the enzyme were used; free and as its cross-linked enzyme aggregate (CLEA). With all substrates, the free enzyme showed activity similar to the CLEA preparation. The advantage of the CLEA phospholipase is the possibility to reuse it in several consecutive reactions without a decrease of activity and selectivity with good but higher yields and ee than with the free enzyme. (author)

  11. Nonnatural amino acid incorporation into the methionine 214 position of the metzincin Pseudomonas aeruginosa alkaline protease

    Directory of Open Access Journals (Sweden)

    Honek John F

    2005-10-01

    Full Text Available Abstract Background The alkaline protease from Pseudomonas aeruginosa (AprA is a member of the metzincin superfamily of metalloendoproteases. A key feature of these proteases is a conserved methionine-containing 1,4-tight β turn at the base of the active site zinc binding region. Results To explore the invariant methionine position in this class of protease, incorporation of a nonnatural fluorinated methionine, L-difluoromethionine (DFM, into this site was accomplished. Although overproduction of the N-terminal catalytic fragment of AprA resulted in protein aggregates which could not be resolved, successful heterologous production of the entire AprA was accomplished in the presence and absence of the nonnatural amino acid. DFM incorporation was found to only slightly alter the enzyme kinetics of AprA. In addition, differential scanning calorimetry indicated no significant alteration in the thermal stability of the modified enzyme. Conclusion Although invariant in all metzincin proteases, the methionine 214 position in AprA can be successfully replaced by the nonnatural amino acid DFM resulting in little effect on protein structure and function. This study indicates that the increased size of the methyl group by the introduction of two fluorines is still sufficiently non-sterically demanding, and bodes well for the application of DFM to biophysical studies of protein structure and function in this class of protease.

  12. Nonnatural amino acid incorporation into the methionine 214 position of the metzincin Pseudomonas aeruginosa alkaline protease

    Science.gov (United States)

    Walasek, Paula; Honek, John F

    2005-01-01

    Background The alkaline protease from Pseudomonas aeruginosa (AprA) is a member of the metzincin superfamily of metalloendoproteases. A key feature of these proteases is a conserved methionine-containing 1,4-tight β turn at the base of the active site zinc binding region. Results To explore the invariant methionine position in this class of protease, incorporation of a nonnatural fluorinated methionine, L-difluoromethionine (DFM), into this site was accomplished. Although overproduction of the N-terminal catalytic fragment of AprA resulted in protein aggregates which could not be resolved, successful heterologous production of the entire AprA was accomplished in the presence and absence of the nonnatural amino acid. DFM incorporation was found to only slightly alter the enzyme kinetics of AprA. In addition, differential scanning calorimetry indicated no significant alteration in the thermal stability of the modified enzyme. Conclusion Although invariant in all metzincin proteases, the methionine 214 position in AprA can be successfully replaced by the nonnatural amino acid DFM resulting in little effect on protein structure and function. This study indicates that the increased size of the methyl group by the introduction of two fluorines is still sufficiently non-sterically demanding, and bodes well for the application of DFM to biophysical studies of protein structure and function in this class of protease. PMID:16221305

  13. Expanding the Enzyme Universe: Accessing Non-Natural Reactions by Mechanism-Guided Directed Evolution

    Science.gov (United States)

    Renata, Hans; Wang, Z. Jane

    2015-01-01

    High selectivities and exquisite control over reaction outcomes entice chemists to use biocatalysts in organic synthesis. However, many useful reactions are not accessible because they are not in nature’s known repertoire. We will use this review to outline an evolutionary approach to engineering enzymes to catalyze reactions not found in nature. We begin with examples of how nature has discovered new catalytic functions and how such evolutionary progressions have been recapitulated in the laboratory starting from extant enzymes. We then examine non-native enzyme activities that have been discovered and exploited for chemical synthesis, emphasizing reactions that do not have natural counterparts. The new functions have mechanistic parallels to the native reaction mechanisms that often manifest as catalytic promiscuity and the ability to convert from one function to the other with minimal mutation. We present examples of how non-natural activities have been improved by directed evolution, mimicking the process used by nature to create new catalysts. Examples of new enzyme functions include epoxide opening reactions with non-natural nucleophiles catalyzed by a laboratory-evolved halohydrin dehalogenase, cyclopropanation and other carbene transfer reactions catalyzed by cytochrome P450 variants, and non-natural modes of cyclization by a modified terpene synthase. Lastly, we describe discoveries of non-native catalytic functions that may provide future opportunities for expanding the enzyme universe. PMID:25649694

  14. Colour agnosia impairs the recognition of natural but not of non-natural scenes.

    Science.gov (United States)

    Nijboer, Tanja C W; Van Der Smagt, Maarten J; Van Zandvoort, Martine J E; De Haan, Edward H F

    2007-03-01

    Scene recognition can be enhanced by appropriate colour information, yet the level of visual processing at which colour exerts its effects is still unclear. It has been suggested that colour supports low-level sensory processing, while others have claimed that colour information aids semantic categorization and recognition of objects and scenes. We investigated the effect of colour on scene recognition in a case of colour agnosia, M.A.H. In a scene identification task, participants had to name images of natural or non-natural scenes in six different formats. Irrespective of scene format, M.A.H. was much slower on the natural than on the non-natural scenes. As expected, neither M.A.H. nor control participants showed any difference in performance for the non-natural scenes. However, for the natural scenes, appropriate colour facilitated scene recognition in control participants (i.e., shorter reaction times), whereas M.A.H.'s performance did not differ across formats. Our data thus support the hypothesis that the effect of colour occurs at the level of learned associations.

  15. Non-natural and photo-reactive amino acids as biochemical probes of immune function.

    Directory of Open Access Journals (Sweden)

    Marta Gómez-Nuñez

    Full Text Available Wilms tumor protein (WT1 is a transcription factor selectively overexpressed in leukemias and cancers; clinical trials are underway that use altered WT1 peptide sequences as vaccines. Here we report a strategy to study peptide-MHC interactions by incorporating non-natural and photo-reactive amino acids into the sequence of WT1 peptides. Thirteen WT1 peptides sequences were synthesized with chemically modified amino acids (via fluorination and photo-reactive group additions at MHC and T cell receptor binding positions. Certain new non-natural peptide analogs could stabilize MHC class I molecules better than the native sequences and were also able to elicit specific T-cell responses and sometimes cytotoxicity to leukemia cells. Two photo-reactive peptides, also modified with a biotin handle for pull-down studies, formed covalent interactions with MHC molecules on live cells and provided kinetic data showing the rapid clearance of the peptide-MHC complex. Despite "infinite affinity" provided by the covalent peptide bonding to the MHC, immunogenicity was not enhanced by these peptides because the peptide presentation on the surface was dominated by catabolism of the complex and only a small percentage of peptide molecules covalently bound to the MHC molecules. This study shows that non-natural amino acids can be successfully incorporated into T cell epitopes to provide novel immunological, biochemical and kinetic information.

  16. Prestorage leukocyte filtration may reduce leukocyte-derived bioactive substance accumulation in patients operated for burn trauma

    DEFF Research Database (Denmark)

    Nielsen, Hans Jørgen; Hammer, J H; Krarup, Annabel Lee

    1999-01-01

    30 min after skin incision until the grafts were secured by wrapping. Samples were also taken 8 h after skin incision and in the morning of postoperative days 1-5. The amount of blood products transfused from admission until day 5 postoperatively was recorded. All patients were followed until......Adverse effects of perioperative blood transfusion appear to be storage-time-dependent and may be related to extracellular accumulation of bioactive substances in blood products. In this study the clinical effects of leukofiltered and non-filtered blood products in patients undergoing surgery...... for burn trauma are investigated. 24 consecutive patients were randomly selected to receive transfusion with non-filtered blood components (group A, n = 12) or similar products, which were prestorage leukofiltered (group B, n = 12). The burn injury was scored using the Bull and Fischer index of age...

  17. Non-natural manners of death among users of illicit drugs: Substance findings.

    Science.gov (United States)

    Delaveris, Gerd Jorunn M; Teige, Brita; Rogde, Sidsel

    2014-05-01

    The aim of the study was to explore differences and similarities between the various non-natural manners of death (accident, suicide, homicide) regarding toxicological findings in illicit drug users. Medicolegal autopsy reports from the Institute of Forensic Medicine University of Oslo concerning deaths from 2000 to 2009 were investigated. Those aged 20-59 whose manner of death was non-natural and who tested positive for any narcotic drug (morphine/heroin, amphetamines, ecstasy, cannabis, LSD, PCP, and high levels of GHB in addition to methadone and buprenorphine) were selected. All substance findings were registered and categorized (narcotics, ethanol, and medicinal products). Of the 1603 autopsies that met the selection criteria, 1204 were accidental intoxications, 122 accidents other than intoxication, 114 suicides by intoxication, 119 non-intoxication suicides, and 44 victims of homicide. Poly drug use was found in all manners of death. The drug profile as well as the mean number of substances (illicit drugs and medicinal products) varied from 2.9 to 4.6 substances per case, depending on the manner of death. Intoxication suicides had the highest number of substances and a total drug profile similar to accidental intoxications. Non-intoxication suicides had a total drug profile similar to homicide and accidents other than intoxication. The number of substances found per case increased during the decade, mainly due to increased findings of methadone, cannabis, amphetamines, and benzodiazepines. Methadone findings increased much more than buprenorphine. Methadone was found 20 times more often than buprenorphine in accidental intoxication cases. In summary, poly drug findings are common in adults who suffer a non-natural death while using illicit drugs. The different manners of death have some specific characteristics and significant differences regarding drug profile. Copyright © 2014 Elsevier Ireland Ltd. All rights reserved.

  18. Energetics and dynamics of the non-natural fluorescent 4AP:DAP base pair

    KAUST Repository

    Chawla, Mohit

    2018-01-02

    The fluorescent non-natural 4-aminophthalimide (4AP) base, when paired to the complementary 2,4-diaminopyrimidine (DAP) nucleobase, is accommodated in a B-DNA duplex being efficiently recognized and incorporated by DNA polymerases. To complement the experimental studies and rationalize the impact of the above non-natural bases on the structure, stability and dynamics of nucleic acid structures, we performed quantum mechanics (QM) calculations along with classical molecular dynamics (MD) simulations. QM calculations were initially focused on the geometry and energetics of the 4AP:DAP non-natural pair and of H-bonded base pairs between 4AP and all the natural bases in their classical Watson-Crick geometries. The QM calculations indicate that the 4AP:DAP pair, despite the fact that it can form 3 H-bonds in a classic Watson-Crick geometry, has a stability comparable to the A:T pair. Then, we extended the study to reverse Watson-Crick geometries, characteristic of parallel strands. MD simulations were carried out on two 13-mer DNA duplexes, featuring a central 4AP:DAP or A:T pair, respectively. No major structural deformation of the duplex was observed during the MD simulation. Snapshots from the MD simulations were subjected to QM calculations to investigate the 4AP:DAP interaction energy when embedded into a duplex structure, and to investigate the impact of the two non-natural bases on the stacking interactions with adjacent bases in the DNA duplex. We found a slight increase in stacking interactions involving the 4AP:DAP pair, counterbalanced by a moderate decrease in H-bonding interactions of the 4AP:DAP and of the adjacent base pairs in the duplex. The results of our study are in agreement with experimental data and complement them by providing an insight into which factors contribute positively and which factors contribute negatively to the structural compatibility of the fluorescent 4AP:DAP pair with a B-DNA structure.

  19. Effect of salivary gland adenocarcinoma cell-derived alpha-N-acetylgalactosaminidase on the bioactivity of macrophage activating factor.

    Science.gov (United States)

    Matsuura, Takashi; Uematsu, Takashi; Yamaoka, Minoru; Furusawa, Kiyofumi

    2004-03-01

    The aim of this study was to clarify the effects of alpha-N-acetylgalactosaminidase (alpha-NaGalase) produced by human salivary gland adenocarcinoma (SGA) cells on the bioactivity of macrophage-activating factor (GcMAF). High exo-alpha-NaGalase activity was detected in the SGA cell line HSG. HSG alpha-NaGalase had both exo- and endo-enzyme activities, cleaving the Gal-GalNAc and GalNAc residues linked to Thr/Ser but not releasing the [NeuAc2-6]GalNac residue. Furthermore, GcMAF enzymatically prepared from the Gc protein enhanced the superoxide-generation capacity and phagocytic activity of monocytes/macrophages. However, GcMAF treated with purified alpha-NaGalase did not exhibit these effects. Thus, HSG possesses the capacity to produce larger quantities of alpha-NaGalase, which inactivates GcMAF produced from Gc protein, resulting in reduced phagocytic activity and superoxide-generation capacity of monocytes/macrophages. The present data strongly suggest that HSG alpha-NaGalase acts as an immunodeficiency factor in cancer patients.

  20. Acid neutralizing, mechanical and physical properties of pit and fissure sealants containing melt-derived 45S5 bioactive glass.

    Science.gov (United States)

    Yang, Song-Yi; Piao, Yin-Zhu; Kim, Sung-Min; Lee, Yong-Keun; Kim, Kyoung-Nam; Kim, Kwang-Mahn

    2013-12-01

    The aim of this study was to examine the effects of 45S5 bioactive glass (BAG) on the acid neutralizing, mechanical and physical properties of pit and fissure sealants. 45S5BAG (glass (180 ± 30 nm) and added into a resin matrix [Bis-GMA/TEGDMA 50/50 (wt%) containing 1% of DMAEMA/CQ 2:1 (wt%)] with varying filler proportions; 0% 45S5BAG+50% glass (BAG0); 12.5% 45S5BAG+37.5% glass (BAG12.5); 25% 45S5BAG+25% glass (BAG25); 37.5% 45S5BAG+12.5% glass (BAG37.5); and 50% 45S5BAG+0% glass (BAG50). To evaluate the acid neutralizing properties, specimens were immersed in lactic acid solution (pH 4.0). Then, the change in pH and the time required to raise the pH from 4.0 to 5.5 were measured. In addition, flexural strength, water sorption and solubility were analyzed. The acid neutralizing properties of each group exhibited increasing pH values as more 45S5BAG was added, and the time required to raise the pH from 4.0 to 5.5 became shorter as the proportion of 45S5BAG increased (P0.05), except for BAG50. The novel pit and fissure sealants neutralized the acid solution (pH 4.0) and exhibited appropriate mechanical and physical properties. Therefore, these compounds are suitable candidates for caries-inhibiting dental materials. Copyright © 2013 Academy of Dental Materials. Published by Elsevier Ltd. All rights reserved.

  1. Characteristics of muscle dysmorphia in male football, weight training, and competitive natural and non-natural bodybuilding samples.

    Science.gov (United States)

    Baghurst, Timothy; Lirgg, Cathy

    2009-06-01

    The purpose of this study was to identify differences in traits associated with muscle dysmorphia between collegiate football players (n=66), weight trainers for physique (n=115), competitive non-natural bodybuilders (n=47), and competitive natural bodybuilders (n=65). All participants completed demographic questionnaires in addition to the Muscle Dysmorphia Inventory (Rhea, Lantz, & Cornelius, 2004). Results revealed a significant main effect for group, and post hoc tests found that the non-natural bodybuilding group did not score significantly higher than the natural bodybuilding group on any subscale except for Pharmacological Use. Both the non-natural and natural bodybuilding groups scored significantly higher than those that weight trained for physique on the Dietary Behavior and Supplement Use subscales. The collegiate football players scored lowest on all subscales of the Muscle Dysmorphia Inventory except for Physique Protection where they scored highest. Findings are discussed with future research expounded.

  2. Development of Emu oil-loaded PCL/collagen bioactive nanofibers for proliferation and stemness preservation of human adipose-derived stem cells: possible application in regenerative medicine.

    Science.gov (United States)

    Nejati-Koshki, Kazem; Pilehvar-Soltanahmadi, Younes; Alizadeh, Effat; Ebrahimi-Kalan, Abbas; Mortazavi, Yousef; Zarghami, Nosratollah

    2017-12-01

    Adipose tissue-derived stem cells (ASCs) are promising candidate in stem cell therapies, and maintaining their stemness potential is vital to achieve effective treatment. Natural-based scaffolds have been recently attracted increasing attention in nanomedicine and drug delivery. In the present study, a polymeric nanofibrous scaffold was developed based on the polycaprolactone/Collagen (PCL/Coll) containing Emu oil as a bioactive material to induce the proliferation of ASCs, while simultaneously preserving the stemness property of those cells. Fabrication of the electrospun Emu oil-loaded PCL/Coll nanofibers was confirmed by using FE-SEM, FTIR, and tensile test. ASCs were seeded on two types of nanofibers (PCL/Coll and Emu oil-loaded PCL/Coll) and their proliferation, cell cycle progression, and stemness gene expressions were evaluated using MTT, propidium iodide staining, and qPCR during 14 days, respectively. The results indicated that ASCs displayed improved adhesion capacity with the higher rates of bioactivity and proliferation on the Emu oil-loaded nanofibers than the other groups. The proliferation capacity of ASCs on Emu oil-loaded PCL/Coll nanofibers was further confirmed by the cell cycle progression analysis. It was also found that Emu oil-loaded nanofibers significantly up-regulated the expression of stemness markers including sox-2, nanog, oct4, klf4, and c-Myc. The results demonstrated that the nanofibers containing Emu oil can reinforce the cell adhesion and enhance ASCs proliferation while preserving their stemness; therefore, using scaffolds containing natural products may have a great potential to enhance the in vitro expansion capacity of ASCs in the field of stem cell therapy and regenerative medicine.

  3. Synthesis, characterization and in vitro bioactivity of sol-gel-derived SiO2-CaO-P2O5-MgO bioglass

    International Nuclear Information System (INIS)

    Saboori, A.; Rabiee, M.; Moztarzadeh, F.; Sheikhi, M.; Tahriri, M.; Karimi, M.

    2009-01-01

    In this study, the synthesis of SiO 2 -CaO-P 2 O 5 -MgO bioactive glass was performed by the sol-gel method. Sol-gel-derived bioglass material was produced both in powder and in discs form by uniaxial pressing, followed by sintering at 700 deg. C. The obtained material was evaluated by X-ray powder diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), scanning electron microscope (SEM), thermal gravimetric analysis (TGA) and differential scanning calorimetry (DSC) analyses. The biocompatibility evaluation of the formed glass was assessed through in vitro cell culture [alkaline phosphatase (AP) activity of osteoblasts] experiments and immersion studies in simulated body fluid (SBF) for different time intervals while monitoring the pH changes and the concentration of calcium, phosphorus and magnesium in the SBF medium. The SEM, XRD and FTIR studies were conducted before and after soaking of the material in SBF. At first, an amorphous calcium phosphate was formed; after 7 days this surface consisted of deposited crystalline apatite. The present investigation also revealed that the sol-gel derived quaternary bioglass system has the ability to support the growth of human fetal osteoblastic cells (hFOB 1.19). Finally, this material proved to be non-toxic and compatible for the proposed work in segmental defects in the goat model in vivo

  4. Bioactive lipid coating of bone allografts directs engraftment and fate determination of bone marrow-derived cells in rat GFP chimeras.

    Science.gov (United States)

    Das, Anusuya; Segar, Claire E; Chu, Yihsuan; Wang, Tiffany W; Lin, Yong; Yang, Chunxi; Du, Xeujun; Ogle, Roy C; Cui, Quanjun; Botchwey, Edward A

    2015-09-01

    Bone grafting procedures are performed to treat wounds incurred during wartime trauma, accidents, and tumor resections. Endogenous mechanisms of repair are often insufficient to ensure integration between host and donor bone and subsequent restoration of function. We investigated the role that bone marrow-derived cells play in bone regeneration and sought to increase their contributions by functionalizing bone allografts with bioactive lipid coatings. Polymer-coated allografts were used to locally deliver the immunomodulatory small molecule FTY720 in tibial defects created in rat bone marrow chimeras containing genetically-labeled bone marrow for monitoring cell origin and fate. Donor bone marrow contributed significantly to both myeloid and osteogenic cells in remodeling tissue surrounding allografts. FTY720 coatings altered the phenotype of immune cells two weeks post-injury, which was associated with increased vascularization and bone formation surrounding allografts. Consequently, degradable polymer coating strategies that deliver small molecule growth factors such as FTY720 represent a novel therapeutic strategy for harnessing endogenous bone marrow-derived progenitors and enhancing healing in load-bearing bone defects. Copyright © 2015 Elsevier Ltd. All rights reserved.

  5. Isovanillin derived N-(un)substituted hydroxylamines possessing an ortho-allylic group: valuable precursors to bioactive N-heterocycles.

    Science.gov (United States)

    Dulla, Balakrishna; Tangellamudi, Neelima D; Balasubramanian, Sridhar; Yellanki, Swapna; Medishetti, Raghavender; Kumar Banote, Rakesh; Hari Chaudhari, Girish; Kulkarni, Pushkar; Iqbal, Javed; Reiser, Oliver; Pal, Manojit

    2014-04-28

    The intramolecular 1,3-dipolar cycloaddition of isovanillin derived N-aryl hydroxylamines possessing ortho-allylic dipolarophiles affords novel benzo analogues of tricyclic isoxazolidines that can be readily transformed into functionalized lactams, γ-aminoalcohols and oxazepines. The corresponding N-unsubstituted hydroxylamines give rise to tetrahydroisoquinolines. Anxiogenic properties of these compounds are tested in zebra fish.

  6. Bioactivity of sol-gel-derived TiO2 coating on polyetheretherketone: In vitro and in vivo studies.

    Science.gov (United States)

    Shimizu, Takayoshi; Fujibayashi, Shunsuke; Yamaguchi, Seiji; Yamamoto, Koji; Otsuki, Bungo; Takemoto, Mitsuru; Tsukanaka, Masako; Kizuki, Takashi; Matsushita, Tomiharu; Kokubo, Tadashi; Matsuda, Shuichi

    2016-04-15

    A polyetheretherketone (PEEK) surface was modified using a sol-gel-derived TiO2 coating in order to confer bone-bonding ability. To enhance the bonding strength of the coating layer, pretreatment with either O2 plasma or sandblasting was performed prior to sol-gel coating. Additionally, post-treatment with acid was carried out to confer apatite (calcium phosphate)-forming ability to the surface. Biomechanical and histological analyses performed using an in vivo rabbit tibia model showed that PEEK surfaces modified with sol-gel-derived TiO2 and acid post-treatment had better bone-bonding properties than uncoated PEEK surfaces. These modified surfaces also performed well in terms of their in vitro cell responses due to their modified surface chemistries and topographies. Although O2 plasma or sandblasting treatment were, for the most part, equivocal in terms of performance, we conclude that sol-gel-derived TiO2 coating followed by acid post-treatment significantly improves the bone bonding ability of PEEK surfaces, thus rendering them optimal for their use in surgical implants. The role of polyetheretherketone (PEEK) as an alternative biomaterial to conventional metallic implant materials has become increasingly important. However, its low bone bonding ability is yet to be resolved. This in vivo and in vitro investigation on the functionalization of PEEK surfaces highlights the utility of this material in clinical interventions that require implants, and may extend range of applications of PEEK. Copyright © 2016 Acta Materialia Inc. Published by Elsevier Ltd. All rights reserved.

  7. Seaweed Bioactivity

    DEFF Research Database (Denmark)

    Zaharudin, Nazikussabah Binti

    . In conclusion, two brown seaweeds, Laminaria digitata and Undaria pinnatifida, inhibited α-amylase and α-glucosidase activities due to their content of several bioactive components with a potential use for future functional foods. Their effects on the postprandial insulin response and the in vitro findings...

  8. Expanding the enzyme universe: accessing non-natural reactions by mechanism-guided directed evolution.

    Science.gov (United States)

    Renata, Hans; Wang, Z Jane; Arnold, Frances H

    2015-03-09

    High selectivity and exquisite control over the outcome of reactions entice chemists to use biocatalysts in organic synthesis. However, many useful reactions are not accessible because they are not in nature's known repertoire. In this Review, we outline an evolutionary approach to engineering enzymes to catalyze reactions not found in nature. We begin with examples of how nature has discovered new catalytic functions and how such evolutionary progression has been recapitulated in the laboratory starting from extant enzymes. We then examine non-native enzyme activities that have been exploited for chemical synthesis, with an emphasis on reactions that do not have natural counterparts. Non-natural activities can be improved by directed evolution, thus mimicking the process used by nature to create new catalysts. Finally, we describe the discovery of non-native catalytic functions that may provide future opportunities for the expansion of the enzyme universe. © 2015 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

  9. CycloPs: generating virtual libraries of cyclized and constrained peptides including nonnatural amino acids.

    Science.gov (United States)

    Duffy, Fergal J; Verniere, Mélanie; Devocelle, Marc; Bernard, Elise; Shields, Denis C; Chubb, Anthony J

    2011-04-25

    We introduce CycloPs, software for the generation of virtual libraries of constrained peptides including natural and nonnatural commercially available amino acids. The software is written in the cross-platform Python programming language, and features include generating virtual libraries in one-dimensional SMILES and three-dimensional SDF formats, suitable for virtual screening. The stand-alone software is capable of filtering the virtual libraries using empirical measurements, including peptide synthesizability by standard peptide synthesis techniques, stability, and the druglike properties of the peptide. The software and accompanying Web interface is designed to enable the rapid generation of large, structurally diverse, synthesizable virtual libraries of constrained peptides quickly and conveniently, for use in virtual screening experiments. The stand-alone software, and the Web interface for evaluating these empirical properties of a single peptide, are available at http://bioware.ucd.ie .

  10. Tools for the identification of bioactives impacting the metabolic syndrome: Screening of a botanical extract library using subcutaneous and visceral human adipose-derived stem cell based assays

    Science.gov (United States)

    Buehrer, Benjamin M.; Duffin, David J.; Lea-Currie, Y. Renee; Ribnicky, David; Raskin, Ilya; Stephens, Jacqueline M.; Cefalu, William T.; Gimble, Jeffrey M.

    2011-01-01

    Plant extracts continue to represent an untapped source of renewable therapeutic compounds for the treatment and prevention of illnesses including chronic metabolic disorders. With the increase in worldwide obesity and its related morbidities, the need for identifying safe and effective treatments is also rising. As such, use of primary human adipose-derived stem cells represents a physiologically relevant cell system to screen for bioactive agents in the prevention and treatment of obesity and its related complications. By using these cells in a primary screen, the risk and cost of identifying artifacts due to interspecies variation and immortalized cell lines is eliminated. We demonstrate that these cells can be formatted into 384-well high throughput screens to rapidly identify botanical extracts that affect lipogenesis and lipolysis. Additionally, counterscreening with human primary stem cells from distinct adipose depots can be routinely performed to identify tissue specific responses. In our study, over 500 botanical extracts were screened and 16 (2.7%) were found to affect lipogenesis and 4 (0.7%) affected lipolysis. PMID:21543201

  11. Chitosan inhibits platelet-mediated clot retraction, increases platelet-derived growth factor release, and increases residence time and bioactivity of platelet-rich plasma in vivo.

    Science.gov (United States)

    Deprés-Tremblay, Gabrielle; Chevrier, Anik; Tran-Khanh, Nicolas; Nelea, Monica; Buschmann, Michael D

    2017-11-10

    Platelet-rich plasma (PRP) has been used to treat different orthopedic conditions, however, the clinical benefits of using PRP remain uncertain. Chitosan (CS)-PRP implants have been shown to improve meniscus, rotator cuff and cartilage repair in pre-clinical models. The purpose of this current study was to investigate in vitro and in vivo mechanisms of action of CS-PRP implants. Freeze-dried formulations containing 1% (w/v) CS (80% degree of deacetylation and number average molar mass 38 kDa), 1% (w/v) trehalose as a lyoprotectant and 42.2 mM calcium chloride as a clot activator were solubilized in PRP. Gravimetric measurements and molecular/cellular imaging studies revealed that clot retraction is inhibited in CS-PRP hybrid clots through physical coating of platelets, blood cells and fibrin strands by chitosan, which interferes with platelet aggregation and platelet-mediated clot retraction. Flow cytometry and ELISA assays revealed that platelets are activated and granules secreted in CS-PRP hybrid clots and that cumulative release of platelet-derived growth factor (PDGF-AB) and epidermal growth factor is higher from CS-PRP hybrid clots compared to PRP clots in vitro. Finally, CS-PRP implants resided for up to 6 weeks in a subcutaneous implantation model and induced cell recruitment and granulation tissue synthesis, confirming greater residency and bioactivity compared to PRP in vivo.

  12. Healthy and adverse effects of plant-derived functional metabolites: the need of revealing their content and bioactivity in a complex food matrix.

    Science.gov (United States)

    Lavecchia, Teresa; Rea, Giuseppina; Antonacci, Amina; Giardi, Maria T

    2013-01-01

    In recent years, both food quality and its effect on human health have become a fundamental issue all over the world. As a consequence of this new and increased awareness, American, European, and Asian policymakers have strongly encouraged the research programs on food quality and safety thematic. Attempts to improve human health and to satisfy people's desire for healthcare without intake of pharmaceuticals, has led the food industry to focus attention on functional or nutraceutical food. For a long time, compounds with nutraceutical activity have been produced chemically, but the new demands for a sustainable life have gradually led the food industry to move towards natural compounds, mainly those derived from plants. Many phytochemicals are known to promote good health, but, sometimes, undesirable effects are also reported. Furthermore, several products present on the market show few benefits and sometimes even the reverse - unhealthy effects; the evidence of efficacy is often unconvincing and epidemiological studies are necessary to prove the truth of their claims. Therefore, there is a need for reliable analytical control systems to measure the bioactivity, content, and quality of these additives in the complex food matrix. This review describes the most widespread nutraceutics and an analytical control of the same using recently developed biosensors which are promising candidates for routine control of functional foods.

  13. The use of embryonic stem cell derived bioactive material as a new protein supplement for the in vitro culture of bovine embryos.

    Science.gov (United States)

    Kim, Eun Young; Lee, Jun Beom; Park, Hyo Young; Jeong, Chang Jin; Riu, Key Zung; Park, Se Pill

    2011-06-01

    Embryonic stem (ES) cells are expanded versions of the inner cell mass cells that compose the early mammalian blastocyst. Components derived from ES cells may contain various bioactive materials (BM) helpful for early preimplantation embryo growth. In this study, we examined the effect of human ES cell derived BM (hES-BM) on in vitro culture of bovine embryos. When bovine parthenogenetic day 2 embryos were cultured in 10% hES-BM, a significantly higher embryo development rate (44.3%) and increased cell numbers were observed relative to control medium containing 3 mg/ml BSA (19.5%; Pculture environment to support the growth of bovine embryos in vitro (P<0.05). Little difference was observed between 10% hES-BM and 10% FBS treatment in the examined parthenogenetic or in vitro fertilized embryos, although the hES-BM group developed at a slightly better rate. However, the ICM cell numbers were significantly higher in the hES-BM group in irrespective of embryo origin (P<0.05). In addition, the relative levels of pluripotency (Oct4, × 1.8 fold; Nanog. × 3.3 fold), embryogenesis (Stat3, × 2.8 fold; FGF4, × 18.8 fold; E-cad, × 2.0 fold) and growth (Glut5, × 2.6 fold) genes were significantly higher in the 10% hES-BM group than in the 10% FBS group (P<0.05), while the levels of other genes (Bax, Bcl2, MnSOD and Connexin43) were not different. This is the first report examining the positive effects of hES-BM on bovine embryo development in vitro. Based on our results, we conclude that hES-BM can be used as a new protein supplement for bovine preimplantation embryo development.

  14. Bioactive effects of graphene oxide cell culture substratum on structure and function of human adipose-derived stem cells.

    Science.gov (United States)

    Kim, Jangho; Choi, Kyoung Soon; Kim, Yeonju; Lim, Ki-Tack; Seonwoo, Hoon; Park, Yensil; Kim, Deok-Ho; Choung, Pill-Hoon; Cho, Chong-Su; Kim, Soo Young; Choung, Yun-Hoon; Chung, Jong Hoon

    2013-12-01

    Nanoscale topography of artificial substrates can greatly influence the fate of stem cells including adhesion, proliferation, and differentiation. Thus the design and manipulation of nanoscale stem cell culture platforms or scaffolds are of great importance as a strategy in stem cell and tissue engineering applications. In this report, we propose that a graphene oxide (GO) film is an efficient platform for modulating structure and function of human adipose-derived stem cells (hASCs). Using a self-assembly method, we successfully coated GO on glass for fabricating GO films. The hASCs grown on the GO films showed increased adhesion, indicated by a large number of focal adhesions, and higher correlation between the orientations of actin filaments and vinculin bands compared to hASCs grown on the glass (uncoated GO substrate). It was also found that the GO films showed the stronger affinity for hASCs than the glass. In addition, the GO film proved to be a suitable environment for the time-dependent viability of hASCs. The enhanced differentiation of hASCs included osteogenesis, adipogenesis, and epithelial genesis, while chondrogenic differentiation of hASCs was decreased, compared to tissue culture polystyrene as a control substrate. The data obtained here collectively demonstrates that the GO film is an efficient substratum for the adhesion, proliferation, and differentiation of hASCs. Copyright © 2013 Wiley Periodicals, Inc., a Wiley Company.

  15. Synthesis and bioactivities of Phenazine-1-carboxylic acid derivatives based on the modification of PCA carboxyl group.

    Science.gov (United States)

    Xiong, Zhipeng; Niu, Junfan; Liu, Hao; Xu, Zhihong; Li, Junkai; Wu, Qinglai

    2017-05-01

    Phenazine-1-carboxylic acid (PCA) as a natural product widely exists in microbial metabolites of Pseudomonads and Streptomycetes and has been registered for the fungicide against rice sheath blight in China. To find higher fungicidal activities compounds and study the effects on fungicidal activities after changing the carboxyl group of PCA, we synthesized a series of PCA derivatives by modifying the carboxyl group of PCA and their structures were confirmed by 1 H NMR and HRMS. Most compounds exhibited significant fungicidal activities in vitro. In particular, compound 6 exhibited inhibition effect against Rhizoctonia solani with EC 50 values of 4.35mg/L and compound 3b exhibited effect against Fusarium graminearum with EC 50 values of 8.30mg/L, compared to the positive control PCA with its EC 50 values of 7.88mg/L (Rhizoctonia solani) and 127.28mg/L (Fusarium graminearum), respectively. The results indicated that the carboxyl group of PCA could be modified to be amide group, acylhydrazine group, ester group, methyl, hydroxymethyl, chloromethyl and ether group etc. And appropriate modifications on carboxyl group of PCA were useful to extend the fungicidal scope. Copyright © 2017 Elsevier Ltd. All rights reserved.

  16. Bioactivity Studies of β-Lactam Derived Polycyclic Fused Pyrroli-Dine/Pyrrolizidine Derivatives in Dentistry: In Vitro, In Vivo and In Silico Studies.

    Directory of Open Access Journals (Sweden)

    Gowri Meiyazhagan

    Full Text Available The antibacterial activity of β-lactam derived polycyclic fused pyrrolidine/pyrrolizidine derivatives synthesized by 1, 3-dipolar cycloaddition reaction was evaluated against microbes involved in dental infection. Fifteen compounds were screened; among them compound 3 showed efficient antibacterial activity in an ex vivo dentinal tubule model and in vivo mice infectious model. In silico docking studies showed greater affinity to penicillin binding protein. Cell damage was observed under Scanning Electron Microscopy (SEM which was further proved by Confocal Laser Scanning Microscope (CLSM and quantified using Flow Cytometry by PI up-take. Compound 3 treated E. faecalis showed ROS generation and loss of membrane integrity was quantified by flow cytometry. Compound 3 was also found to be active against resistant E. faecalis strains isolated from failed root canal treatment cases. Further, compound 3 was found to be hemocompatible, not cytotoxic to normal mammalian NIH 3T3 cells and non mutagenic. It was concluded that β-lactam compound 3 exhibited promising antibacterial activity against E. faecalis involved in root canal infections and the mechanism of action was deciphered. The results of this research can be further implicated in the development of potent antibacterial medicaments with applications in dentistry.

  17. Bioactivity Studies of β-Lactam Derived Polycyclic Fused Pyrroli-Dine/Pyrrolizidine Derivatives in Dentistry: In Vitro, In Vivo and In Silico Studies

    Science.gov (United States)

    Winfred, Sofi Beaula; Mannivanan, Bhavani; Bhoopalan, Hemadev; Shankar, Venkatesh; Sekar, Sathiya; Venkatachalam, Deepa Parvathi; Pitani, Ravishankar; Nagendrababu, Venkateshbabu; Thaiman, Malini; Devivanayagam, Kandaswamy; Jayaraman, Jeyakanthan; Ragavachary, Raghunathan; Venkatraman, Ganesh

    2015-01-01

    The antibacterial activity of β-lactam derived polycyclic fused pyrrolidine/pyrrolizidine derivatives synthesized by 1, 3-dipolar cycloaddition reaction was evaluated against microbes involved in dental infection. Fifteen compounds were screened; among them compound 3 showed efficient antibacterial activity in an ex vivo dentinal tubule model and in vivo mice infectious model. In silico docking studies showed greater affinity to penicillin binding protein. Cell damage was observed under Scanning Electron Microscopy (SEM) which was further proved by Confocal Laser Scanning Microscope (CLSM) and quantified using Flow Cytometry by PI up-take. Compound 3 treated E. faecalis showed ROS generation and loss of membrane integrity was quantified by flow cytometry. Compound 3 was also found to be active against resistant E. faecalis strains isolated from failed root canal treatment cases. Further, compound 3 was found to be hemocompatible, not cytotoxic to normal mammalian NIH 3T3 cells and non mutagenic. It was concluded that β-lactam compound 3 exhibited promising antibacterial activity against E. faecalis involved in root canal infections and the mechanism of action was deciphered. The results of this research can be further implicated in the development of potent antibacterial medicaments with applications in dentistry. PMID:26185985

  18. Computational Design of Non-natural Sugar Alcohols to Increase Thermal Storage Density: Beyond Existing Organic Phase Change Materials.

    Science.gov (United States)

    Inagaki, Taichi; Ishida, Toyokazu

    2016-09-14

    Thermal storage, a technology that enables us to control thermal energy, makes it possible to reuse a huge amount of waste heat, and materials with the ability to treat larger thermal energy are in high demand for energy-saving societies. Sugar alcohols are now one promising candidate for phase change materials (PCMs) because of their large thermal storage density. In this study, we computationally design experimentally unknown non-natural sugar alcohols and predict their thermal storage density as a basic step toward the development of new high performance PCMs. The non-natural sugar alcohol molecules are constructed in silico in accordance with the previously suggested molecular design guidelines: linear elongation of a carbon backbone, separated distribution of OH groups, and even numbers of carbon atoms. Their crystal structures are then predicted using the random search method and first-principles calculations. Our molecular simulation results clearly demonstrate that the non-natural sugar alcohols have potential ability to have thermal storage density up to ∼450-500 kJ/kg, which is significantly larger than the maximum thermal storage density of the present known organic PCMs (∼350 kJ/kg). This computational study suggests that, even in the case of H-bonded molecular crystals where the electrostatic energy contributes mainly to thermal storage density, the molecular distortion and van der Waals energies are also important factors to increase thermal storage density. In addition, the comparison between the three eight-carbon non-natural sugar alcohol isomers indicates that the selection of preferable isomers is also essential for large thermal storage density.

  19. Nonnatural deaths among users of illicit drugs: pathological findings and illicit drug abuse stigmata.

    Science.gov (United States)

    Delaveris, Gerd Jorunn Møller; Hoff-Olsen, Per; Rogde, Sidsel

    2015-03-01

    The aim of the study was to provide information on illicit drug abuse stigmata and general pathological findings among an adult narcotic drug-using population aged 20 to 59 years whose death was nonnatural. A total of 1603 medicolegal autopsy reports from 2000 to 2009 concerning cases positive for morphine, heroin, amphetamines, ecstasy, cannabis, LSD (lysergic acid diethylamide), PCP (phencyclidine), and high levels of GHB (γ-hydroxybutyric acid) in addition to methadone and buprenorphine were investigated. Reported findings of hepatitis, portal lymphadenopathy, recent injection marks, drug user's equipment, and numbers of significant pathological conditions were registered and analyzed according to cases positive for opiates, opioids (OPs), and central nervous system (CNS)-stimulating illicit drugs, respectively. Of the selected cases, 1305 were positive for one or more opiate or OP. Cases positive for OPs had significantly more findings of noninfectious pathological conditions. Hepatitis, portal lymphadenopathy, recent injections marks findings of drug user's equipment were all findings found more frequently among the opiate OP-positive individuals. Portal lymphadenopathy was significantly more often found in cases with hepatitis than in cases with other or no infection. In the population positive for CNS stimulants, hepatitis recent injection marks were more frequent findings than in the CNS stimulant-negative group, irrespective of whether they were opiate OP positive or negative.

  20. Nonnatural deaths of children under the age of 5 years in Ontario, Canada: A retrospective autopsy analysis of 10 years (2006-2015

    Directory of Open Access Journals (Sweden)

    Syeda Sakina Rizvi

    2017-01-01

    Full Text Available The goal of this study is to unravel the common patterns observed among nonnatural deaths of children under 5 years and suggest ways to prevent such unnecessary deaths. The study was confined to the province of Ontario to allow the identification of regional specific patterns. The database at the Office of the Chief Coroner of Ontario was searched for all pediatric deaths from the years 2006-2015. All nonnatural deaths for children under the age of 5 years, including sudden infant death syndrome, were selected for the study. Manner and cause of death along with the corresponding year were recorded in tables. In the 10-year period, 940 nonnatural deaths were identified in Ontario through autopsy records which are equal to approximately 36.7% of the total childhood deaths. There were 295 accidental cases (11.6% and 71 homicides (2.8%. The leading causes of nonnatural childhood deaths in Ontario were drowning, traffic accidents, blunt trauma, and asphyxia. Nonnatural deaths are preventable through education and training of parents. Implementation of educational interventions can significantly reduce nonnatural deaths of children in Ontario.

  1. Comparative metabolism of [14C]benzene to excretable products and bioactivation to DNA-binding derivatives in maternal and neonatal mice

    International Nuclear Information System (INIS)

    Iba, M.M.; Ghosal, A.; Snyder, R.

    2001-01-01

    Lactating adult female mice treated with a single dose of 880 mg/kg i.p. [ 14 C]benzene, and their 2-day-old sucklings similarly treated or nursed by their treated dams were compared in terms of their ability to metabolize benzene to urinary products or reactive intermediates as assessed by covalently-bound benzene derivatives in whole blood or liver DNA. Six metabolite fractions were identified in the urine of sucklings by high performance liquid chromatographic (HPLC) analysis at 5 h following intraperitoneal (direct) treatment with benzene. Three of the metabolite fractions co-chromatographed with authentic phenol, phenyl glucuronide, and muconic acid, and contributed 11, 6.9 and 0.6%, respectively, to the total urinary benzene metabolites. Two of the fractions were unidentified. The sixth and most polar fraction consisted of multiple metabolites, 21% of which were conjugates, and accounted for 72% of the total urinary metabolites. A similar metabolite profile was observed in 24-h urine samples from treated dams with the exception that one of the unidentified fractions in the sucklings was absent and levels of the metabolites were quantitatively higher than those observed in sucklings 5 h following their treatment with benzene. Furthermore, 78% of the most polar fraction from the dams consisted of conjugates compared with 21% of that from the sucklings. The metabolite pattern in urine of sucklings nursed by treated dams was qualitatively similar to, but quantitatively different from the pattern in treated dams. Five hours following intraperitoneal treatment with benzene, covalent binding of the compound to DNA (expressed as pmol benzene equivalents/mg DNA) in sucklings was slightly higher in whole blood (1.15±0.07) than in liver (0.77±0.07), whereas in the dam, it was slightly lower in whole blood (0.88±0.48) than in liver (1.63±0.61). Twenty four hours following benzene exposure in sucklings of benzene-treated dams, DNA binding by the compound in whole

  2. Accurate Dereplication of Bioactive Secondary Metabolites from Marine-Derived Fungi by UHPLC-DAD-QTOFMS and a MS/HRMS Library

    DEFF Research Database (Denmark)

    Kildgaard, Sara; Mansson, Maria; Dosen, Ina

    2014-01-01

    In drug discovery, reliable and fast dereplication of known compounds is essential for identification of novel bioactive compounds. Here, we show an integrated approach using ultra-high performance liquid chromatography-diode array detection-quadrupole time of flight mass spectrometry (UHPLC-DAD-...

  3. Mixed protocols: Multiple ratios of FSH and LH bioactivity using highly purified, human-derived FSH (BRAVELLE and highly purified hMG (MENOPUR are unaltered by mixing together in the same syringe

    Directory of Open Access Journals (Sweden)

    Raike Elizabeth

    2005-11-01

    Full Text Available Abstract Background The use of mixed or blended protocols, that utilize both FSH and hMG, for controlled ovarian hyperstimulation is increasing in use. To reduce the number of injections a patient must administer, many physicians instruct their patients to mix their FSH and hMG together to be given as a single injection. Therefore, the goal of this study was to definitively determine if the FSH and LH bioactivities of highly purified, human-derived FSH (Bravelle(R and highly purified hMG (Menopur(R were altered by reconstituting in 0.9% saline and mixing in the same syringe. Methods Bravelle(R and Menopur(R were reconstituted in 0.9% saline and mixed in a Becton Dickinson plastic syringe. The FSH and LH bioactivities of the products were determined after injecting female and male rats, respectively, with Bravelle(R, Menopur(R, or a mixture of Bravelle(R and Menopur(R. Ratios of FSH:LH activity tested were 150:75 IU (1 vial Bravelle(R: 1 vial Menopur(R, 300:75 IU (3 vials Bravelle(R: 1 vial Menopur(R or 300:225 IU (1 vial Bravelle(R: 3 vials of Menopur(R. Results There were no statistically significant changes in either FSH or LH bioactivity that occurred after mixing Bravelle(R with Menopur(R in the same syringe. The theoretical vs. actual FSH bioactivity for Bravelle(R and Menopur(R were 75 vs. 76.58 IU/mL and 75 vs. 76.0 IU/mL, respectively. For the 3 ratios of FSH:LH activity tested, 150:75 IU (1 vial Bravelle(R: 1 vial Menopur(R, 300:75 IU (3 vials Bravelle(R: 1 vial Menopur(R or 300:225 IU (1 vial Bravelle(R: 3 vials of Menopur(R tested, the theoretical vs. actual FSH bioactivities were 150 vs. 156.86 IU/mL, 300 vs. 308.69 IU/mL and 300 vs. 306.58 IU/mL, respectively. The theoretical vs. actual LH bioactivity for Menopur(R in the above mentioned ratios tested were 75 vs. 77.50 IU/mL. For the 3 ratios of FSH:LH activity tested, 150:75 IU (1 vial Bravelle(R: 1 vial Menopur(R, 300:75 IU (3 vials Bravelle(R: 1 vial Menopur(R or 300:225 IU (1

  4. Effect of magnesia on the degradability and bioactivity of sol-gel derived SiO2-CaO-MgO-P2O5 system glasses.

    Science.gov (United States)

    Ma, J; Chen, C Z; Wang, D G; Jiao, Y; Shi, J Z

    2010-11-01

    Mesoporous 58SiO(2)-(38-x)CaO-xMgO-4P(2)O(5) glasses (where x=0, 5, 10 and 20 mol%) have been prepared by the sol-gel synthesis route. The effects of the substitution of MgO for CaO on glass degradation and bioactivity were studied in tris-(hydroxymethyl)-aminomethane and hydrochloric acid buffer solution (Tris-HCl) and simulated body fluid (SBF), respectively. It is observed that the synthesized glasses with various MgO contents possess the similar textural properties. The studies of in vitro degradability and bioactivity show that the rate of glass degradation gradually decreases with the increase of MgO and the formation of apatite layer on glass surface is retarded. The influences of the composition upon glass properties are explained in terms of their internal structures. Copyright (c) 2010 Elsevier B.V. All rights reserved.

  5. Micro-ion beam analysis of physico-chemical reactions in vitro induced by nano-structured sol-gel derived bioactive glasses

    International Nuclear Information System (INIS)

    Lao, J.

    2007-07-01

    The study of bioactive glasses is a multi-field area of research aiming at a major goal: the development of new generation biomaterials that would be able to bond with host tissues through the formation of a strong interfacial bond, together with helping the body heal itself through the stimulation of specific cellular responses. Thus clinical applications of bioactive glasses mainly concern dental surgery and orthopedics, for filling osseous defects. For this purpose, we have elaborated bioactive glasses in the binary SiO 2 -CaO system, ternary SiO 2 -CaO-P 2 O 5 system, and for the first time, to our knowledge, strontium-doped SiO 2 -CaO-SrO and SiO 2 -CaO-P 2 O 5 -SrO glasses. The materials were elaborated using the sol-gel process, which allowed the synthesis of nano-porous materials with great purity and homogeneity. The bio-activity of the glasses was clearly demonstrated in vitro: in contact with biological fluids, the whole lot of mate-rials were able to induce the formation of a Ca-P-Mg layer a few microns thick at their surface. Our work is characterized by the use of PIXE-RBS nuclear microprobes to study the bioactive glass/biological fluids interface. Thanks to these methods we obtained chemical maps that made possible the analysis of major and trace elements concentrations at the interface. Moreover, quantitative information regarding the local reactivity of glasses were acquired. These data are important to evaluate the kinetics and amplitude of the physico-chemical reactions involved in the bio-activity process. Thus, we highlighted that the binary glass is the highest reactive regarding the dissolution of the glassy matrix as well as the first appearance of the Ca-P rich layer. However the Ca/P atomic ratio calculated at the glass/biological fluids interface decreases slowly, indicating that the Ca-P-Mg layer encounters difficulties to be changed into a more stable apatitic phase. For the P-containing glasses, the de-alkalinization of the matrix and

  6. Investigation of Seismic Waves from Non-Natural Sources: A Case Study for Building Collapse and Surface Explosion

    Science.gov (United States)

    Houng, S.; Hong, T.

    2013-12-01

    The nature and excitation mechanism of incidents or non-natural events have been widely investigated using seismological techniques. With introduction of dense seismic networks, small-sized non-natural events such as building collapse and chemical explosions are well recorded. Two representative non-natural seismic sources are investigated. A 5-story building in South Korea, Sampoong department store, was collapsed in June 25, 1995, causing casualty of 1445. This accident is known to be the second deadliest non-terror-related building collapse in the world. The event was well recorded by a local station in ~ 9 km away. P and S waves were recorded weak, while monotonic Rayleigh waves were observed well. The origin time is determined using surface-wave arrival time. The magnitude of event is determined to be 1.2, which coincides with a theoretical estimate based on the mass and volume of building. Synthetic waveforms are modeled for various combinations of velocity structures and source time functions, which allow us to constrain the process of building collapse. It appears that the building was collapsed once within a couple of seconds. We also investigate a M2.1 chemical explosion at a fertilizer plant in Texas on April 18, 2013. It was reported that more than one hundred people were dead or injured by the explosion. Seismic waveforms for nearby stations are collected from Incorporated Research Institution of Seismology (IRIS). The event was well recorded at stations in ~500 km away from the source. Strong acoustic signals were observed at stations in a certain great-circle direction. This observation suggests preferential propagation of acoustic waves depending on atmospheric environment. Waveform cross-correlation, spectral analysis and waveform modeling are applied to understand the source physics. We discuss the nature of source and source excitation mechanism.

  7. In vitro solubility and bioactivity of Sr and Mg co-doped calcium phosphate glass-ceramics derived from different heat-treatment temperatures

    International Nuclear Information System (INIS)

    Cai Shu; Li Jianxin; Xu Guohua; Li, Xudong; Ye Xiaojian; Jiang Wei

    2011-01-01

    Highlights: ► Porous glass ceramics were prepared by controlled heat treatment process. ► A fast release of Mg ions has a great influence on the Ca/P ratio of the deposits. ► The chemical stability of the deposited apatite directly affects cell behavior. ► The glass ceramics heat-treated at 760 °C and 780 °C show less glass. ► The degradation rates are both compatible with cell growth and differentiation. - Abstract: CaO–P 2 O 5 –Na 2 O–SrO–MgO glass–ceramic system was prepared by controlled heat treatment process. Solubility and bioactivity of glass-ceramics were measured and evaluated in simulated body fluid (SBF) and cell culture medium respectively. The dissolution behavior of these glass-ceramics strongly depends on the amount and microstructure of the crystals precipitated by sintering treatment. Concerning the bioactivity, the onset of the apatite formation on the glass–ceramic system was directly dependent on the amount of bioactive glass amount which can be controlled using different temperatures of heat treatment. After immersing glass–ceramic in SBF, Mg ion as one of system composition can be released from residual glass and provides a high impact on the Ca/P ratio and chemical stability of the deposited apatite layer that directly affects cell attachment and proliferation in in vitro cell culture system. The glass ceramics heat-treated at 760 °C and 780 °C show less glass amount, and their degradation rates are both compatible with cell growth and differentiation.

  8. Prevalence of prescription and illicit drugs in pregnancy-associated non-natural deaths of Florida mothers, 1999-2005.

    Science.gov (United States)

    Hardt, Nancy; Wong, Tit D; Burt, Martha J; Harrison, Ross; Winter, Will; Roth, Jeffrey

    2013-11-01

    Abuse of prescription and illicit drugs has been rapidly increasing. This study examines the prevalence of drug use in the non-natural deaths of pregnant or recently pregnant women. Records from Florida's Pregnancy Associated Mortality Review conducted between 1999 and 2005 (n = 415) were linked to 385 toxicology reports obtained from Florida medical examiners' offices. The final study sample consisted of 169 drug-positive, pregnancy-associated non-natural deaths. Of these, 86 were positive for both blood and urine, 64 were positive for blood only and five for urine only, and the remainder were positive for some other specimen. Among these deaths, 91 cases (54%) involved prescription drugs, 78 cases (46%) involved illicit drugs, and 69 cases (41%) involved alcohol. Opioids constituted the majority of deaths associated with prescription drugs. Substantial co-use of opioids and benzodiazepines was seen. Pregnant or recently pregnant women may have more interactions with healthcare providers, which may present more opportunities for intervention and prevention. © 2013 American Academy of Forensic Sciences.

  9. New Insight into the Cleavage Reaction of Nostoc sp. Strain PCC 7120 Carotenoid Cleavage Dioxygenase in Natural and Nonnatural Carotenoids

    Science.gov (United States)

    Heo, Jinsol; Kim, Se Hyeuk

    2013-01-01

    Carotenoid cleavage dioxygenases (CCDs) are enzymes that catalyze the oxidative cleavage of carotenoids at a specific double bond to generate apocarotenoids. In this study, we investigated the activity and substrate preferences of NSC3, a CCD of Nostoc sp. strain PCC 7120, in vivo and in vitro using natural and nonnatural carotenoid structures. NSC3 cleaved β-apo-8′-carotenal at 3 positions, C-13C-14, C-15C-15′, and C-13′C-14′, revealing a unique cleavage pattern. NSC3 cleaves the natural structure of carotenoids 4,4′-diaponeurosporene, 4,4′-diaponeurosporen-4′-al, 4,4′-diaponeurosporen-4′-oic acid, 4,4′-diapotorulene, and 4,4′-diapotorulen-4′-al to generate novel cleavage products (apo-14′-diaponeurosporenal, apo-13′-diaponeurosporenal, apo-10′-diaponeurosporenal, apo-14′-diapotorulenal, and apo-10′-diapotorulenal, respectively). The study of carotenoids with natural or nonnatural structures produced by using synthetic modules could provide information valuable for understanding the cleavage reactions or substrate preferences of other CCDs in vivo and in vitro. PMID:23524669

  10. In vitro response of human osteoblasts to multi-step sol–gel derived bioactive glass nanoparticles for bone tissue engineering

    International Nuclear Information System (INIS)

    Fan, Jian Ping; Kalia, Priya; Di Silvio, Lucy; Huang, Jie

    2014-01-01

    A multi-step sol–gel process was employed to synthesize bioactive glass (BG) nanoparticles. Transmission electron microscopy (TEM) revealed that the BG nanoparticles were spherical and ranged from 30 to 60 nm in diameter. In vitro reactivity of the BG nanoparticles was tested in phosphate buffer saline (PBS), Tris-buffer (TRIS), simulated body fluid (SBF), and Dulbecco's modified Eagle's medium (DMEM), in comparison with similar sized hydroxyapatite (HA) and silicon substituted HA (SiHA) nanoparticles. Bioactivity of the BG nanoparticles was confirmed through Fourier transform infrared spectroscopy (FTIR) analysis. It was found that bone-like apatite was formed after immersion in SBF at 7 days. Solutions containing BG nanoparticles were slightly more alkaline than HA and SiHA, suggesting that a more rapid apatite formation on BG was related to solution-mediated dissolution. Primary human osteoblast (HOB) cell model was used to evaluate biological responses to BG nanoparticles. Lactate dehydrogenase (LDH) cytotoxicity assay showed that HOB cells were not adversely affected by the BG nanoparticles throughout the 7 day test period. Interestingly, MTS assay results showed an enhancement in cell proliferation in the presence of BG when compared to HA and SiHA nanoparticles. Particularly, statistically significant (p < 0.05) alkaline phosphatase (ALP) activity of HOB cells was found on the culture containing BG nanoparticles, suggesting that the cell differentiation might be promoted by BG. Real-time quantitative PCR analysis (qPCR) further confirmed this finding, as a significantly higher level of RUNX2 gene expression was recorded on the cells cultured in the presence of BG nanoparticles when compared to those with HA and SiHA. - Highlights: • Spherical bioactive glass nanoparticles (BG) under 60 nm were synthesized. • An alkali morphological catalyst was used in the synthesis. • Cytotoxicity assays demonstrated that BG was not cytotoxic towards HOB

  11. Sol-gel-derived bioactive glass nanoparticle-incorporated glass ionomer cement with or without chitosan for enhanced mechanical and biomineralization properties.

    Science.gov (United States)

    Kim, Dong-Ae; Lee, Jung-Hwan; Jun, Soo-Kyung; Kim, Hae-Won; Eltohamy, Mohamed; Lee, Hae-Hyoung

    2017-07-01

    This study investigated the mechanical and in vitro biological properties (in immortalized human dental pulp stem cells (ihDPSCs)) of bioactive glass nanoparticle (BGN)-incorporated glass ionomer cement (GIC) with or without chitosan as a binder. After the BGNs were synthesized and characterized, three experimental GICs and a control (conventional GIC) that differed in the additive incorporated into a commercial GIC liquid (Hy-bond, Shofu, Japan) were produced: BG5 (5wt% of BGNs), CL0.5 (0.5wt% of chitosan), and BG5+CL0.5 (5wt% of BGNs and 0.5wt% of chitosan). After the net setting time was determined, weight change and bioactivity were analyzed in simulated body fluid (SBF) at 37°C. Mechanical properties (compressive strength, diametral tensile strength, flexural strength and modulus) were measured according to the incubation time (up to 28 days) in SBF. Cytotoxicity (1day) and biomineralization (14 days), assessed by alizarin red staining, were investigated using an extract from GIC and ihDPSCs. Data were analyzed using one-way analysis of variance (ANOVA) followed by Tukey's post hoc test; pproperties were increased in the BGN-incorporated GICs compared to those in the control (pproperties such as compressive, diametral tensile and flexural strength as well as in vitro biomineralization properties in ihDPSCs without cytotoxicity. Therefore, the developed BGN-incorporated GIC is a promising restorative dental material, although further in vivo investigation is needed before clinical application. Copyright © 2017 The Academy of Dental Materials. Published by Elsevier Ltd. All rights reserved.

  12. Easy design of colorimetric logic gates based on nonnatural base pairing and controlled assembly of gold nanoparticles.

    Science.gov (United States)

    Zhang, Li; Wang, Zhong-Xia; Liang, Ru-Ping; Qiu, Jian-Ding

    2013-07-16

    Utilizing the principles of metal-ion-mediated base pairs (C-Ag-C and T-Hg-T), the pH-sensitive conformational transition of C-rich DNA strand, and the ligand-exchange process triggered by DL-dithiothreitol (DTT), a system of colorimetric logic gates (YES, AND, INHIBIT, and XOR) can be rationally constructed based on the aggregation of the DNA-modified Au NPs. The proposed logic operation system is simple, which consists of only T-/C-rich DNA-modified Au NPs, and it is unnecessary to exquisitely design and alter the DNA sequence for different multiple molecular logic operations. The nonnatural base pairing combined with unique optical properties of Au NPs promises great potential in multiplexed ion sensing, molecular-scale computers, and other computational logic devices.

  13. Marine Peptides: Bioactivities and Applications

    Directory of Open Access Journals (Sweden)

    Randy Chi Fai Cheung

    2015-06-01

    Full Text Available Peptides are important bioactive natural products which are present in many marine species. These marine peptides have high potential nutraceutical and medicinal values because of their broad spectra of bioactivities. Their antimicrobial, antiviral, antitumor, antioxidative, cardioprotective (antihypertensive, antiatherosclerotic and anticoagulant, immunomodulatory, analgesic, anxiolytic anti-diabetic, appetite suppressing and neuroprotective activities have attracted the attention of the pharmaceutical industry, which attempts to design them for use in the treatment or prevention of various diseases. Some marine peptides or their derivatives have high commercial values and had reached the pharmaceutical and nutraceutical markets. A large number of them are already in different phases of the clinical and preclinical pipeline. This review highlights the recent research in marine peptides and the trends and prospects for the future, with special emphasis on nutraceutical and pharmaceutical development into marketed products.

  14. Maize Bioactive Peptides against Cancer

    Science.gov (United States)

    Díaz-Gómez, Jorge L.; Castorena-Torres, Fabiola; Preciado-Ortiz, Ricardo E.; García-Lara, Silverio

    2017-06-01

    Cancer is one of the main chronic degenerative diseases worldwide. In recent years, consumption of whole-grain cereals and their derived food products has been associated with reduction risks of various types of cancer. Cereals main biomolecules includes proteins, peptides, and amino acids present in different quantities within the grain. The nutraceutical properties associated with peptides exerts biological functions that promote health and prevent this disease. In this review, we report the current status and advances on maize peptides regarding bioactive properties that have been reported such as antioxidant, antihypertensive, hepatoprotective, and anti-tumour activities. We also highlighted its biological potential through which maize bioactive peptides exert anti-cancer activity. Finally, we analyse and emphasize the possible areas of application for maize peptides.

  15. Bioactivity and cell proliferation in radiopaque gel-derived CaO-P2O5-SiO2-ZrO2 glass and glass-ceramic powders.

    Science.gov (United States)

    Montazerian, Maziar; Yekta, Bijan Eftekhari; Marghussian, Vahak Kaspari; Bellani, Caroline Faria; Siqueira, Renato Luiz; Zanotto, Edgar Dutra

    2015-10-01

    In this study, 10 mol% ZrO2 was added to a 27CaO-5P2O5-68SiO2 (mol%) base composition synthesized via a simple sol-gel method. This composition is similar to that of a frequently investigated bioactive gel-glass. The effects of ZrO2 on the in vitro bioactivity and MG-63 cell proliferation of the glass and its derivative polycrystalline (glass-ceramic) powder were investigated. The samples were characterized using thermo-gravimetric and differential thermal analysis (TG/DTA), X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), and scanning electron microscopy (SEM) coupled to energy dispersive X-ray spectroscopy (EDS). Release of Si, Ca, P and Zr into simulated body fluid (SBF) was determined by inductively coupled plasma (ICP). Upon heat treatment at 1000 °C, the glass powder crystallized into an apatite-wollastonite-zirconia glass-ceramic powder. Hydroxycarbonate apatite (HCA) formation on the surface of the glass and glass-ceramic particles containing ZrO2 was confirmed by FTIR and SEM. Addition of ZrO2 to the base glass composition decreased the rate of HCA formation in vitro from one day to three days, and hence, ZrO2 could be employed to control the rate of apatite formation. However, the rate of HCA formation on the glass-ceramic powder containing ZrO2 crystal was equal to that in the base glassy powder. Tests with a cultured human osteoblast-like MG-63 cells revealed that the glass and glass-ceramic materials stimulated cell proliferation, indicating that they are biocompatible and are not cytotoxic in vitro. Moreover, zirconia clearly increased osteoblast proliferation over that of the Zr-free samples. This increase is likely associated with the lower solubility of these samples and, consequently, a smaller variation in the media pH. Despite the low solubility of these materials, bioactivity was maintained, indicating that these glassy and polycrystalline powders are potential candidates for bone graft substitutes and bone cements with

  16. The human VGF-derived bioactive peptide TLQP-21 binds heat shock 71 kDa protein 8 (HSPA8on the surface of SH-SY5Y cells.

    Directory of Open Access Journals (Sweden)

    Shamim Akhter

    Full Text Available VGF (non-acronymicis a secreted chromogranin/secretogranin that gives rise to a number of bioactive peptides by a complex proteolysis mechanism. VGF-derived peptides exert an extensive array of biological effects in energy metabolism, mood regulation, pain, gastric secretion function, reproduction and, perhaps, cancer. It is therefore surprising that very little is known about receptors and binding partners of VGF-derived peptides and their downstream molecular mechanisms of action. Here, using affinity chromatography and mass spectrometry-based protein identification, we have identified the heat shock cognate 71 kDa protein A8 (HSPA8as a binding partner of human TLQP-21 on the surface of human neuroblastomaSH-SY5Y cells. Binding of TLQP-21 to membrane associated HSPA8 in live SH-SY5Y cells was further supported by cross-linking to live cells. Interaction between HSPA8 and TLQP-21 was confirmed in vitro by label-free Dynamic Mass Redistribution (DMR studies. Furthermore, molecular modeling studies show that TLQP-21 can be docked into the HSPA8 peptide binding pocket. Identification of HSPA8 as a cell surface binding partner of TLQP-21 opens new avenues to explore the molecular mechanisms of its physiological actions, and of pharmacological modulation thereof.

  17. Bioactive proteins from pipefishes

    Directory of Open Access Journals (Sweden)

    E. Rethna Priya

    2013-01-01

    Full Text Available Objective: To screen antimicrobial potence of some pipefish species collected from Tuticorin coastal environment. Methods: Antimicrobial activity of pipefishes in methanol extract was investigated against 10 bacterial and 10 fungal human pathogenic strains. Results: Among the tested strains, in Centriscus scutatus, pipefish showed maximum zone of inhibition against Vibrio cholerae (8 mm and minimum in the sample of Hippichthys cyanospilos against Klebseilla pneumoniae (2 mm. In positive control, maximum zone of inhibition was recorded in Vibrio cholerae (9 mm and minimum in Klebseilla pneumoniae, and Salmonella paratyphi (5 mm. Chemical investigation indicated the presence of peptides as evidenced by ninhydrin positive spots on thin layer chromatography and presence of peptide. In SDS PAGE, in Centriscus scutatus, four bands were detected in the gel that represented the presence of proteins in the range nearly 25.8-75 kDa. In Hippichthys cyanospilos, five bands were detected in the gel that represented the presence of proteins in the range nearly 20.5-78 kDa. The result of FT-IR spectrum revealed that the pipe fishes extracts compriseed to have peptide derivatives as their predominant chemical groups. Conclusions: It can be conclude that this present investigation suggests the tested pipe fishes will be a potential source of natural bioactive compounds.

  18. Bioactive proteins from pipefishes

    Directory of Open Access Journals (Sweden)

    E. Rethna Priya

    2013-08-01

    Full Text Available Objective: To screen antimicrobial potence of some pipefish species collected from Tuticorin coastal environment. Methods: Antimicrobial activity of pipefishes in methanol extract was investigated against 10 bacterial and 10 fungal human pathogenic strains. Results: Among the tested strains, in Centriscus scutatus, pipefish showed maximum zone of inhibition against Vibrio cholerae (8 mm and minimum in the sample of Hippichthys cyanospilos against Klebseilla pneumoniae (2 mm. In positive control, maximum zone of inhibition was recorded in Vibrio cholerae (9 mm and minimum in Klebseilla pneumoniae, and Salmonella paratyphi (5 mm. Chemical investigation indicated the presence of peptides as evidenced by ninhydrin positive spots on thin layer chromatography and presence of peptide. In SDS PAGE, in Centriscus scutatus, four bands were detected in the gel that represented the presence of proteins in the range nearly 25.8-75 kDa. In Hippichthys cyanospilos, five bands were detected in the gel that represented the presence of proteins in the range nearly 20.5-78 kDa. The result of FT-IR spectrum revealed that the pipe fishes extracts compriseed to have peptide derivatives as their predominant chemical groups. Conclusions: It can be conclude that this present investigation suggests the tested pipe fishes will be a potential source of natural bioactive compounds.

  19. Platelet-rich plasma and its derivatives as promising bioactive materials for regenerative medicine: basic principles and concepts underlying recent advances.

    Science.gov (United States)

    Kawase, Tomoyuki

    2015-05-01

    Over the past decade, platelet-rich plasma (PRP), a platelet-concentrated plasma fraction, has been widely investigated and applied to regenerative medicine. The clinical utility of PRP is supported by evidence that PRP contains high concentrations of platelet-related growth factors and normal concentrations of plasma-derived fibrinogen, both of which contribute synergistically to the regenerative process. Additionally, its superior cost-efficacy versus conventional therapies is attractive to many clinicians. However, current disadvantages of PRP include a relatively complicated preparation procedure and variable operator-dependent efficacy. An additional disadvantage is the use of bovine thrombin, an animal-derived biological, as a coagulant. Many of these disadvantages are overcome by recent advances in preparation procedures and devices; for example, Joseph Choukroun simplified the platelet-rich fibrin preparation procedure and improved handling efficiency without the aid of animal-derived factors. With advancements in cell processing technology, there has been a general shift in cell therapy from autologous to allogeneic treatment; however, autologous PRP therapy will not easily be replaced by allogeneic treatment in the near future. Therefore, to provide more predictable regenerative therapy outcomes using autologous PRP, further investigations should address developing a standardized procedure for PRP preparation to augment its efficacy and potency, independent of donor variability. We would then propose that operators and clinicians prepare PRP according to the standardized protocol and to carefully evaluate the clinical scenario (i.e., recipient factors comprising skeletal defects) to determine which factor(s) should be added to PRP preparations. This careful approach will lead to improved clinical outcomes for patients.

  20. Comparative Proteomic Characterization of 4 Human Liver-Derived Single Cell Culture Models Reveals Significant Variation in the Capacity for Drug Disposition, Bioactivation, and Detoxication.

    Science.gov (United States)

    Sison-Young, Rowena L C; Mitsa, Dimitra; Jenkins, Rosalind E; Mottram, David; Alexandre, Eliane; Richert, Lysiane; Aerts, Hélène; Weaver, Richard J; Jones, Robert P; Johann, Esther; Hewitt, Philip G; Ingelman-Sundberg, Magnus; Goldring, Christopher E P; Kitteringham, Neil R; Park, B Kevin

    2015-10-01

    In vitro preclinical models for the assessment of drug-induced liver injury (DILI) are usually based on cryopreserved primary human hepatocytes (cPHH) or human hepatic tumor-derived cell lines; however, it is unclear how well such cell models reflect the normal function of liver cells. The physiological, pharmacological, and toxicological phenotyping of available cell-based systems is necessary in order to decide the testing purpose for which they are fit. We have therefore undertaken a global proteomic analysis of 3 human-derived hepatic cell lines (HepG2, Upcyte, and HepaRG) in comparison with cPHH with a focus on drug metabolizing enzymes and transport proteins (DMETs), as well as Nrf2-regulated proteins. In total, 4946 proteins were identified, of which 2722 proteins were common across all cell models, including 128 DMETs. Approximately 90% reduction in expression of cytochromes P450 was observed in HepG2 and Upcyte cells, and approximately 60% in HepaRG cells relative to cPHH. Drug transporter expression was also lower compared with cPHH with the exception of MRP3 and P-gp (MDR1) which appeared to be significantly expressed in HepaRG cells. In contrast, a high proportion of Nrf2-regulated proteins were more highly expressed in the cell lines compared with cPHH. The proteomic database derived here will provide a rational basis for the context-specific selection of the most appropriate 'hepatocyte-like' cell for the evaluation of particular cellular functions associated with DILI and, at the same time, assist in the construction of a testing paradigm which takes into account the in vivo disposition of a new drug. © The Author 2015. Published by Oxford University Press on behalf of the Society of Toxicology.

  1. Stabilization of Angiotensin-(1-7) by key substitution with a cyclic non-natural amino acid.

    Science.gov (United States)

    Wester, Anita; Devocelle, Marc; Tallant, E Ann; Chappell, Mark C; Gallagher, Patricia E; Paradisi, Francesca

    2017-10-01

    Angiotensin-(1-7) [Ang-(1-7)], a heptapeptide hormone of the renin-angiotensin-aldosterone system, is a promising candidate as a treatment for cancer that reflects its anti-proliferative and anti-angiogenic properties. However, the peptide's therapeutic potential is limited by the short half-life and low bioavailability resulting from rapid enzymatic metabolism by peptidases including angiotensin-converting enzyme (ACE) and dipeptidyl peptidase 3 (DPP 3). We report the facile assembly of three novel Ang-(1-7) analogues by solid-phase peptide synthesis which incorporates the cyclic non-natural δ-amino acid ACCA. The analogues containing the ACCA substitution at the site of ACE cleavage exhibit complete resistance to human ACE, while substitution at the DDP 3 cleavage site provided stability against DPP 3 hydrolysis. Furthermore, the analogues retain the anti-proliferative properties of Ang-(1-7) against the 4T1 and HT-1080 cancer cell lines. These results suggest that ACCA-substituted Ang-(1-7) analogues which show resistance against proteolytic degradation by peptidases known to hydrolyze the native heptapeptide may be novel therapeutics in the treatment of cancer.

  2. Selective fluorescence resonance energy transfer from serum albumins to a bio-active 3-pyrazolyl-2-pyrazoline derivative: A spectroscopic analysis

    Energy Technology Data Exchange (ETDEWEB)

    Sarkar, Arindam [Department of Chemistry, Jadavpur University, Kolkata 700032 (India); Bhattacharya, Subhash Chandra, E-mail: sbjuchem@yahoo.com [Department of Chemistry, Jadavpur University, Kolkata 700032 (India)

    2012-10-15

    A novel fluorescent probe and pharmaceutically significant: 3-pyrazolyl-2-pyrazoline derivative (PYZ) has been selected as an acceptor molecule for fluorescence resonance energy transfer (FRET) interaction with serum albumins. Steady state and time resolved fluorescence techniques were applied to elucidate the nature of interaction of PYZ with serum albumins (BSA and HSA). Negligible FRET mediated emission occurred in the case of HSA but an efficient FRET mediated emission resulted in case of BSA. To gain further insight into the FRET selectivity of PYZ with the proteins, FRET from L-tryptophan (donor; native tryptophan) to PYZ (acceptor) was performed with the aim of getting an idea about the steric restrictions imposed on PYZ by the other groups present in BSA and HSA. The studies revealed that the surface bound Trp-134 in BSA allows an efficient FRET process with PYZ while the buried Trp-214 in HSA does not. The unusual selectivity for FRET in case of PYZ and the serum albumins has also been attributed to the complex structure of PYZ due to the presence of bulkier phenyl moieties in it. The complex nature of the excited state photophysics of tryptophan (Trp) in proteins also accounts for this FRET selectivity of PYZ with BSA and HSA. - Highlights: Black-Right-Pointing-Pointer FRET from BSA/HSA to PYZ was monitored using steady state and time resolved fluorescence methods. Black-Right-Pointing-Pointer Efficient FRET process resulted in BSA-PYZ system in contrast with the HSA-PYZ system. Black-Right-Pointing-Pointer Surface bound Trp-134 in BSA facilitates the FRET process with PYZ than the buried Trp-214 in HSA. Black-Right-Pointing-Pointer Rigid and complex structure of PYZ also accounts for the FRET selectivity of PYZ with BSA/HSA.

  3. Influence of Mussel-Derived Bioactive BMP-2-Decorated PLA on MSC Behavior in Vitro and Verification with Osteogenicity at Ectopic Sites in Vivo.

    Science.gov (United States)

    Chen, Zhuoyue; Zhang, Zhen; Feng, Juantao; Guo, Yayuan; Yu, Yuan; Cui, Jihong; Li, Hongmin; Shang, Lijun

    2018-04-11

    Osteoinductive activity of the implant in bone healing and regeneration is still a challenging research topic. Therapeutic application of recombinant human bone morphogenetic protein-2 (BMP-2) is a promising approach to enhance osteogenesis. However, high dose and uncontrolled burst release of BMP-2 may introduce edema, bone overgrowth, cystlike bone formation, and inflammation. In this study, low-dose BMP-2 of 1 μg was used to design PLA-PD-BMP for functionalization of polylactic acid (PLA) implants via mussel-inspired polydopamine (PD) assist. For the first time, the binding property and efficiency of the PD coating with BMP-2 were directly demonstrated and analyzed using an antigen-antibody reaction. The obtained PLA-PD-BMP surface immobilized with this low BMP-2 dose can endow the implants with abilities of introducing strong stem cell adhesion and enhanced osteogenicity. Furthermore, in vivo osteoinduction of the PLA-PD-BMP-2 scaffolds was confirmed by a rat ectopic bone model, which is marked as the "gold standard" for the evidence of osteoinductive activity. The microcomputed tomography, Young's modulus, and histology analyses were also employed to demonstrate that PLA-PD-BMP grafted with 1 μg of BMP-2 can induce bone formation. Therefore, the method in this study can be used as a model system to immobilize other growth factors onto various different types of polymer substrates. The highly biomimetic mussel-derived strategy can therefore improve the clinical outcome of polymer-based medical implants in a facile, safe, and effective way.

  4. Structure, bioactivity, and synthesis of methylated flavonoids.

    Science.gov (United States)

    Wen, Lingrong; Jiang, Yueming; Yang, Jiali; Zhao, Yupeng; Tian, Miaomiao; Yang, Bao

    2017-06-01

    Methylated flavonoids are an important type of natural flavonoid derivative with potentially multiple health benefits; among other things, they have improved bioavailability compared with flavonoid precursors. Flavonoids have been documented to have broad bioactivities, such as anticancer, immunomodulation, and antioxidant activities, that can be elevated, to a certain extent, by methylation. Understanding the structure, bioactivity, and bioavailability of methylated flavonoids, therefore, is an interesting topic with broad potential applications. Though methylated flavonoids are widely present in plants, their levels are usually low. Because developing efficient techniques to produce these chemicals would likely be beneficial, we provide an overview of their chemical and biological synthesis. © 2017 New York Academy of Sciences.

  5. Detection of non-natural springtime precipitation change over northern South America

    Science.gov (United States)

    Barkhordarian, A.; Behrangi, A.; Mechoso, C. R.

    2017-12-01

    Here we determine whether the climate over South America has changed as a result of human activity since the beginning of the industrial revolution. To this end, we assess whether the observed changes are likely to have been due to natural (internal) variability alone, and if not, whether they are consistent with what models simulate as response to anthropogenic and natural forcing. Internal variability is estimated using 12,000-year control runs derived from CMIP5 archive. Results indicate that, in the past decades, trends in springtime (ASO, August-October) precipitation over South America have a magnitude that is beyond the estimated range due to natural (internal) variability or natural forcings alone. Evidence for the presence of an external driving factor is clearly detectable in the observed precipitation record (with less than 5% risk of error). The regression results illustrate the concerted emergence of an anthropogenic signal consistent with greenhouse gas (GHG) in observed decreasing 30-year trends of precipitation ending in 1998 and later on. In addition, the fingerprint of land-use-change signal is detectable in the observed precipitation decrease over 1983-2012. While the influence of GHG signal is detectable in precipitation, an observed decrease up to 10 mm/decade drying over the Amazon region, is much larger than the changes simulated by global and regional climate models as response to GHG forcing. We further show that the projected increasing trend of vapor pressure deficit (VPD), an indicator of background aridity, by the climate models with GHG forcing is much smaller than that observed over the Amazon rainforest. This may imply that models may underestimate the resulting reductions in forest CO2 uptake that could function as a positive feedback to rising temperature and reducing precipitation. Taking the ensemble of 23 IPCC models as a crude metric of probabilities, we further show that with 19 out of 24 models the effect of GS signal

  6. Bioavailability of bioactive food compounds: a challenging journey to bioefficacy

    Science.gov (United States)

    Rein, Maarit J.; Renouf, Mathieu; Cruz‐Hernandez, Cristina; Actis‐Goretta, Lucas; Thakkar, Sagar K.; da Silva Pinto, Marcia

    2013-01-01

    Bioavailability is a key step in ensuring bioefficacy of bioactive food compounds or oral drugs. Bioavailability is a complex process involving several different stages: liberation, absorption, distribution, metabolism and elimination phases (LADME). Bioactive food compounds, whether derived from various plant or animal sources, need to be bioavailable in order to exert any beneficial effects. Through a better understanding of the digestive fate of bioactive food compounds we can impact the promotion of health and improvement of performance. Many varying factors affect bioavailability, such as bioaccessibility, food matrix effect, transporters, molecular structures and metabolizing enzymes. Bioefficacy may be improved through enhanced bioavailability. Therefore, several technologies have been developed to improve the bioavailability of xenobiotics, including structural modifications, nanotechnology and colloidal systems. Due to the complex nature of food bioactive compounds and also to the different mechanisms of absorption of hydrophilic and lipophilic bioactive compounds, unravelling the bioavailability of food constituents is challenging. Among the food sources discussed during this review, coffee, tea, citrus fruit and fish oil were included as sources of food bioactive compounds (e.g. (poly)phenols and polyunsaturated fatty acids (PUFAs)) since they are examples of important ingredients for the food industry. Although there are many studies reporting on bioavailability and bioefficacy of these bioactive food components, understanding their interactions, metabolism and mechanism of action still requires extensive work. This review focuses on some of the major factors affecting the bioavailability of the aforementioned bioactive food compounds. PMID:22897361

  7. Bioactive focus in conformational ensembles: a pluralistic approach

    Science.gov (United States)

    Habgood, Matthew

    2017-12-01

    Computational generation of conformational ensembles is key to contemporary drug design. Selecting the members of the ensemble that will approximate the conformation most likely to bind to a desired target (the bioactive conformation) is difficult, given that the potential energy usually used to generate and rank the ensemble is a notoriously poor discriminator between bioactive and non-bioactive conformations. In this study an approach to generating a focused ensemble is proposed in which each conformation is assigned multiple rankings based not just on potential energy but also on solvation energy, hydrophobic or hydrophilic interaction energy, radius of gyration, and on a statistical potential derived from Cambridge Structural Database data. The best ranked structures derived from each system are then assembled into a new ensemble that is shown to be better focused on bioactive conformations. This pluralistic approach is tested on ensembles generated by the Molecular Operating Environment's Low Mode Molecular Dynamics module, and by the Cambridge Crystallographic Data Centre's conformation generator software.

  8. Nanoencapsulation of bioactive compounds for food applications

    OpenAIRE

    Sessa, Mariarenata

    2012-01-01

    2010 - 2011 The increase in dietary-intake-related illnesses, such as obesity, cardiovascular diseases, hypertension, diabetes and cancer, have made in recent years the development of health-and-wellness promoting foods a priority of the food industry. Clinical studies have demonstrated tangible health benefits that may be derived from the intake of bioactive compounds. However many difficulties are associated with their inclusion in food matrices, due to a very low solubility in water and...

  9. Bioactive polymeric scaffolds for tissue engineering

    Directory of Open Access Journals (Sweden)

    Scott Stratton

    2016-12-01

    Full Text Available A variety of engineered scaffolds have been created for tissue engineering using polymers, ceramics and their composites. Biomimicry has been adopted for majority of the three-dimensional (3D scaffold design both in terms of physicochemical properties, as well as bioactivity for superior tissue regeneration. Scaffolds fabricated via salt leaching, particle sintering, hydrogels and lithography have been successful in promoting cell growth in vitro and tissue regeneration in vivo. Scaffold systems derived from decellularization of whole organs or tissues has been popular due to their assured biocompatibility and bioactivity. Traditional scaffold fabrication techniques often failed to create intricate structures with greater resolution, not reproducible and involved multiple steps. The 3D printing technology overcome several limitations of the traditional techniques and made it easier to adopt several thermoplastics and hydrogels to create micro-nanostructured scaffolds and devices for tissue engineering and drug delivery. This review highlights scaffold fabrication methodologies with a focus on optimizing scaffold performance through the matrix pores, bioactivity and degradation rate to enable tissue regeneration. Review highlights few examples of bioactive scaffold mediated nerve, muscle, tendon/ligament and bone regeneration. Regardless of the efforts required for optimization, a shift in 3D scaffold uses from the laboratory into everyday life is expected in the near future as some of the methods discussed in this review become more streamlined.

  10. Applied bioactive polymeric materials

    CERN Document Server

    Carraher, Charles; Foster, Van

    1988-01-01

    The biological and biomedical applications of polymeric materials have increased greatly in the past few years. This book will detail some, but not all, of these recent developments. There would not be enough space in this book to cover, even lightly, all of the major advances that have occurred. Some earlier books and summaries are available by two of this book's Editors (Gebelein & Carraher) and these should be consul ted for additional information. The books are: "Bioactive Polymeric Systems" (Plenum, 1985); "Polymeric Materials In Medication" (Plenum, 1985); "Biological Acti vi ties of Polymers" (American Chemical Society, 1982). Of these three, "Bioacti ve Polymeric Systems" should be the most useful to a person who is new to this field because it only contains review articles written at an introductory level. The present book primarily consists of recent research results and applications, with only a few review or summary articles. Bioactive polymeric materials have existed from the creation of life...

  11. Bioactive technologies for hemocompatibility.

    Science.gov (United States)

    Tanzi, Maria Cristina

    2005-07-01

    The contact of any biomaterial with blood gives rise to multiple pathophysiologic defensive mechanisms such as activation of the coagulation cascade, platelet adhesion and activation of the complement system and leukocytes. The reduction of these events is of crucial importance for the successful clinical performance of a cardiovascular device. This can be achieved by improving the hemocompatibility of the device materials or by pharmacologic inhibition of the key enzymes responsible for the activation of the cascade reactions, or a combination of both. Different strategies have been developed during the last 20 years, and this article attempts to review the most significant, by dividing them into three main categories: bioinert or biopassive, biomimetic and bioactive strategies. With regard to bioactive strategies, particular attention is given to heparin immobilization and recent related technologies. References from both scientific literature and commercial sites are provided. Future development and studies are suggested.

  12. Bioactive glass in tissue engineering

    Science.gov (United States)

    Rahaman, Mohamed N.; Day, Delbert E.; Bal, B. Sonny; Fu, Qiang; Jung, Steven B.; Bonewald, Lynda F.; Tomsia, Antoni P.

    2011-01-01

    This review focuses on recent advances in the development and use of bioactive glass for tissue engineering applications. Despite its inherent brittleness, bioactive glass has several appealing characteristics as a scaffold material for bone tissue engineering. New bioactive glasses based on borate and borosilicate compositions have shown the ability to enhance new bone formation when compared to silicate bioactive glass. Borate-based bioactive glasses also have controllable degradation rates, so the degradation of the bioactive glass implant can be more closely matched to the rate of new bone formation. Bioactive glasses can be doped with trace quantities of elements such as Cu, Zn and Sr, which are known to be beneficial for healthy bone growth. In addition to the new bioactive glasses, recent advances in biomaterials processing have resulted in the creation of scaffold architectures with a range of mechanical properties suitable for the substitution of loaded as well as non-loaded bone. While bioactive glass has been extensively investigated for bone repair, there has been relatively little research on the application of bioactive glass to the repair of soft tissues. However, recent work has shown the ability of bioactive glass to promote angiogenesis, which is critical to numerous applications in tissue regeneration, such as neovascularization for bone regeneration and the healing of soft tissue wounds. Bioactive glass has also been shown to enhance neocartilage formation during in vitro culture of chondrocyte-seeded hydrogels, and to serve as a subchondral substrate for tissue-engineered osteochondral constructs. Methods used to manipulate the structure and performance of bioactive glass in these tissue engineering applications are analyzed. PMID:21421084

  13. Meat and fermented meat products as a source of bioactive peptides.

    Science.gov (United States)

    Stadnik, Joanna; Kęska, Paulina

    2015-01-01

    Bioactive peptides are short amino acid sequences, that upon release from the parent protein may play different physiological roles, including antioxidant, antihypertensive, antimicrobial, and other bioactivities. They have been identified from a range of foods, including those of animal origin, e.g., milk and muscle sources (with pork, beef, or chicken and various species of fish and marine organism). Bioactive peptides are encrypted within the sequence of the parent protein molecule and latent until released and activated by enzymatic proteolysis, e.g. during gastrointestinal digestion or food processing. Bioactive peptides derived from food sources have the potential for incorporation into functional foods and nutraceuticals. The aim of this paper is to present an overview of the muscle-derived bioactive peptides, especially those of fermented meats and the potential benefits of these bioactive compounds to human health.

  14. Analysis of commercial and public bioactivity databases.

    Science.gov (United States)

    Tiikkainen, Pekka; Franke, Lutz

    2012-02-27

    Activity data for small molecules are invaluable in chemoinformatics. Various bioactivity databases exist containing detailed information of target proteins and quantitative binding data for small molecules extracted from journals and patents. In the current work, we have merged several public and commercial bioactivity databases into one bioactivity metabase. The molecular presentation, target information, and activity data of the vendor databases were standardized. The main motivation of the work was to create a single relational database which allows fast and simple data retrieval by in-house scientists. Second, we wanted to know the amount of overlap between databases by commercial and public vendors to see whether the former contain data complementing the latter. Third, we quantified the degree of inconsistency between data sources by comparing data points derived from the same scientific article cited by more than one vendor. We found that each data source contains unique data which is due to different scientific articles cited by the vendors. When comparing data derived from the same article we found that inconsistencies between the vendors are common. In conclusion, using databases of different vendors is still useful since the data overlap is not complete. It should be noted that this can be partially explained by the inconsistencies and errors in the source data.

  15. Bioactive Lipids in Dairy Fat

    DEFF Research Database (Denmark)

    Hellgren, Lars; Nordby, Pernille

    2017-01-01

    Milk fat is the most important energy source for the newborn infant beside its important role as energy source, milk fat also contain a range of bioactive lipids, that potentially can modulate the immune response and metabolic regulation in the child. In this chapter we review the literature on b...... on bioactive dairy fatty acids: conjugated linoleic acid, branched chained and odd chained fatty acids, as well as bioactive complex lipids such as sphingomyelin and gangliosides....

  16. Bioactive materials for biomedical applications using sol-gel technology

    International Nuclear Information System (INIS)

    Gupta, Radha; Kumar, Ashok

    2008-01-01

    This review paper focuses on the sol-gel technology that has been applied in many of the potential research areas and highlights the importance of sol-gel technology for preparing bioactive materials for biomedical applications. The versatility of sol-gel chemistry enables us to manipulate the characteristics of material required for particular applications. Sol-gel derived materials have proved to be good biomaterials for coating films and for the construction of super-paramagnetic nanoparticles, bioactive glasses and fiberoptic applicators for various biomedical applications. The introduction of the sol-gel route in a conventional method of preparing implants improves the mechanical strength, biocompatibility and bioactivity of scaffolds and prevents corrosion of metallic implants. The use of organically modified silanes (ORMOSILS) yields flexible and bioactive materials for soft and hard tissue replacement. A novel approach of nitric-oxide-releasing sol-gels as antibacterial coatings for reducing the infection around orthopedic implants has also been discussed

  17. Bioactive lipids in kidney physiology and pathophysiology

    Directory of Open Access Journals (Sweden)

    Daria Sałata

    2014-01-01

    Full Text Available Lipids not only have structural functions, but also play an important role as signaling and regulatory molecules and participate in many cellular processes such as proliferation, differentiation, migration, and apoptosis. Bioactive lipids act both as extracellular mediators, which are associated with receptors on the surface of cells, and intracellular mediators triggering different signal pathways. They are present and active in physiological conditions, and are also involved in the pathogenesis of inflammation, asthma, cancer, diabetes, and hypertension. Bioactive lipids such as derivatives of arachidonic acid and sphingolipids have an important role in renal development, physiology and in many renal diseases. Some of them are potential indicators of kidney damage degree and/or function of the transplanted kidneys.

  18. Broad spectrum bioactive sunscreens.

    Science.gov (United States)

    Velasco, Maria Valéria Robles; Sarruf, Fernanda Daud; Salgado-Santos, Idalina Maria Nunes; Haroutiounian-Filho, Carlos Alberto; Kaneko, Telma Mary; Baby, André Rolim

    2008-11-03

    The development of sunscreens containing reduced concentration of chemical UV filters, even though, possessing broad spectrum effectiveness with the use of natural raw materials that improve and infer UV absorption is of great interest. Due to the structural similarities between polyphenolic compounds and organic UV filters, they might exert photoprotection activity. The objective of the present research work was to develop bioactive sunscreen delivery systems containing rutin, Passiflora incarnata L. and Plantago lanceolata extracts associated or not with organic and inorganic UV filters. UV transmission of the sunscreen delivery system films was performed by using diffuse transmittance measurements coupling to an integrating sphere. In vitro photoprotection efficacy was evaluated according to the following parameters: estimated sun protection factor (SPF); Boot's Star Rating category; UVA/UVB ratio; and critical wavelength (lambda(c)). Sunscreen delivery systems obtained SPF values ranging from 0.972+/-0.004 to 28.064+/-2.429 and bioactive compounds interacted with the UV filters positive and negatively. This behavior may be attributed to: the composition of the delivery system; the presence of inorganic UV filter and quantitative composition of the organic UV filters; and the phytochemical composition of the P. incarnata L. and P. lanceolata extracts. Among all associations of bioactive compounds and UV filters, we found that the broad spectrum sunscreen was accomplished when 1.68% (w/w) P. incarnata L. dry extract was in the presence of 7.0% (w/w) ethylhexyl methoxycinnamate, 2.0% (w/w) benzophenone-3 and 2.0% (w/w) TiO(2). It was demonstrated that this association generated estimated SPF of 20.072+/-0.906 and it has improved the protective defense against UVA radiation accompanying augmentation of the UVA/UVB ratio from 0.49 to 0.52 and lambda(c) from 364 to 368.6nm.

  19. LASER-INDUCED BIOACTIVITY IN DENTAL PORCELAIN MODIFIED BY BIOACTIVE GLASS

    Directory of Open Access Journals (Sweden)

    ANASTASIA BEKETOVA

    2012-12-01

    Full Text Available The aim of this study was to investigate the impact of laser-liquid-solid interaction method in the bioactivity of dental porcelain modified by bioactive glass. Forty sol-gel derived specimens were immersed in Dulbecco's Modified Eagle's Medium, 31 and 9 specimens of which were treated with Er:YAG and Nd:YAG laser respectively. Untreated specimens served as controls. Incubation of specimens followed. Bioactivity was evaluated, using Fourier Transform Infrared spectroscopy (FTIR, Scanning Electron Microscopy (SEM/Energy Dispersive Spectroscopy (EDS and Transmission Electron Microscopy (TEM. FTIR detected peaks associated with hydroxyapatite on 1 Nd:YAG- and 4 Er:YAG-treated specimens. SEM analysis revealed that Er:YAG-treated specimens were covered by granular hydroxyapatite layer, while Nd:YAG treated specimen presented growth of flake-like hydroxyapatite. TEM confirmed the results. The untreated controls presented delayed bioactivity. In conclusion, Nd:YAG and Er:YAG laser treatment of the material, under certain fluencies, accelerates hydroxyapatite formation. Nd:YAG laser treatment of specific parameters causes the precipitation of flake-like hydroxyapatite in nano-scale.

  20. Nanotech: propensity in foods and bioactives.

    Science.gov (United States)

    Kuan, Chiu-Yin; Yee-Fung, Wai; Yuen, Kah-Hay; Liong, Min-Tze

    2012-01-01

    Nanotechnology is seeing higher propensity in various industries, including food and bioactives. New nanomaterials are constantly being developed from both natural biodegradable polymers of plant and animal origins such as polysaccharides and derivatives, peptides and proteins, lipids and fats, and biocompatible synthetic biopolyester polymers such as polylactic acid (PLA), polyhydroxyalkonoates (PHA), and polycaprolactone (PCL). Applications in food industries include molecular synthesis of new functional food compounds, innovative food packaging, food safety, and security monitoring. The relevance of bioactives includes targeted delivery systems with improved bioavailability using nanostructure vehicles such as association colloids, lipid based nanoencapsulator, nanoemulsions, biopolymeric nanoparticles, nanolaminates, and nanofibers. The extensive use of nanotechnology has led to the need for parallel safety assessment and regulations to protect public health and adverse effects to the environment. This review covers the use of biopolymers in the production of nanomaterials and the propensity of nanotechnology in food and bioactives. The exposure routes of nanoparticles, safety challenges, and measures undertaken to ensure optimal benefits that outweigh detriments are also discussed.

  1. Bioavailability of bioactive food compounds: a challenging journey to bioefficacy.

    Science.gov (United States)

    Rein, Maarit J; Renouf, Mathieu; Cruz-Hernandez, Cristina; Actis-Goretta, Lucas; Thakkar, Sagar K; da Silva Pinto, Marcia

    2013-03-01

    Bioavailability is a key step in ensuring bioefficacy of bioactive food compounds or oral drugs. Bioavailability is a complex process involving several different stages: liberation, absorption, distribution, metabolism and elimination phases (LADME). Bioactive food compounds, whether derived from various plant or animal sources, need to be bioavailable in order to exert any beneficial effects. Through a better understanding of the digestive fate of bioactive food compounds we can impact the promotion of health and improvement of performance. Many varying factors affect bioavailability, such as bioaccessibility, food matrix effect, transporters, molecular structures and metabolizing enzymes. Bioefficacy may be improved through enhanced bioavailability. Therefore, several technologies have been developed to improve the bioavailability of xenobiotics, including structural modifications, nanotechnology and colloidal systems. Due to the complex nature of food bioactive compounds and also to the different mechanisms of absorption of hydrophilic and lipophilic bioactive compounds, unravelling the bioavailability of food constituents is challenging. Among the food sources discussed during this review, coffee, tea, citrus fruit and fish oil were included as sources of food bioactive compounds (e.g. (poly)phenols and polyunsaturated fatty acids (PUFAs)) since they are examples of important ingredients for the food industry. Although there are many studies reporting on bioavailability and bioefficacy of these bioactive food components, understanding their interactions, metabolism and mechanism of action still requires extensive work. This review focuses on some of the major factors affecting the bioavailability of the aforementioned bioactive food compounds. © 2012 Nestec S. A.. British Journal of Clinical Pharmacology © 2012 The British Pharmacological Society.

  2. Towards the synthesis of an experimental bioactive dental ceramic. Part I: Crystallinity characterization and bioactive behavior evaluation

    Energy Technology Data Exchange (ETDEWEB)

    Goudouri, O.-M. [Physics Department, Aristotle University of Thessaloniki, 54124 Thessaloniki (Greece); Kontonasaki, E. [School of Dentistry, Aristotle University of Thessaloniki, 54124 Thessaloniki (Greece); Papadopoulou, L.; Kantiranis, N. [Department of Geology, Aristotle University of Thessaloniki, 54124 Thessaloniki (Greece); Lazaridis, N.K. [Chemistry Department, Aristotle University of Thessaloniki, 54124 Thessaloniki (Greece); Chrissafis, K.; Chatzistavrou, X. [Physics Department, Aristotle University of Thessaloniki, 54124 Thessaloniki (Greece); Koidis, P. [School of Dentistry, Aristotle University of Thessaloniki, 54124 Thessaloniki (Greece); Paraskevopoulos, K.M., E-mail: kpar@auth.gr [Physics Department, Aristotle University of Thessaloniki, 54124 Thessaloniki (Greece)

    2014-05-01

    An attachment between the dental ceramic and the surrounding marginal tissues in fixed prosthetic restorations could eliminate secondary carries prevalence. The development of dental ceramics with apatite forming ability could provide the biological surface required for selective spread and attachment of specific cell types able to promote tissue attachment. Dental ceramics/bioactive glass composites synthesized by the sol gel method have been previously reported to develop carbonated hydroxyapatite (HCAp) in biomimetic solutions, requiring though a high amount of bioactive glass, which resulted in the compromise of their mechanical integrity. Thus, the aim of the present work was the synthesis and characterization of an experimental sol–gel derived dental ceramic with low amount of bioactive glass and the evaluation of its in vitro bioactivity. Differential thermal and thermogravimetric analysis (TG–DTA), Fourier Transform Infrared Spectroscopy (FTIR), X-ray Diffractometry (XRD), Scanning Electron Microscopy (SEM) and Energy Dispersive Spectroscopy (EDS) were used to evaluate the crystal structure and the in vitro apatite forming ability of the synthesized material. The results of this study indicated the successful sol–gel synthesis of an experimental dental ceramic containing low amount of bioactive glass that presented similar structural and morphological characteristics with a commercial feldspathic dental ceramic, while exhibiting in vitro bioactivity. The apatite forming ability of the experimental sol–gel derived feldspathic dental ceramic may trigger the appropriate cellular mechanisms towards the establishment of attachment with the surrounding connective tissue. This attachment could provide a barrier to oral bacteria penetration, prolonging the life expectation of the restorations. - Highlights: • Synthesis of a bioactive sol–gel dental ceramic for fixed prosthetic restorations. • The sol–gel technique promoted the crystallization of

  3. Towards the synthesis of an experimental bioactive dental ceramic. Part I: Crystallinity characterization and bioactive behavior evaluation

    International Nuclear Information System (INIS)

    Goudouri, O.-M.; Kontonasaki, E.; Papadopoulou, L.; Kantiranis, N.; Lazaridis, N.K.; Chrissafis, K.; Chatzistavrou, X.; Koidis, P.; Paraskevopoulos, K.M.

    2014-01-01

    An attachment between the dental ceramic and the surrounding marginal tissues in fixed prosthetic restorations could eliminate secondary carries prevalence. The development of dental ceramics with apatite forming ability could provide the biological surface required for selective spread and attachment of specific cell types able to promote tissue attachment. Dental ceramics/bioactive glass composites synthesized by the sol gel method have been previously reported to develop carbonated hydroxyapatite (HCAp) in biomimetic solutions, requiring though a high amount of bioactive glass, which resulted in the compromise of their mechanical integrity. Thus, the aim of the present work was the synthesis and characterization of an experimental sol–gel derived dental ceramic with low amount of bioactive glass and the evaluation of its in vitro bioactivity. Differential thermal and thermogravimetric analysis (TG–DTA), Fourier Transform Infrared Spectroscopy (FTIR), X-ray Diffractometry (XRD), Scanning Electron Microscopy (SEM) and Energy Dispersive Spectroscopy (EDS) were used to evaluate the crystal structure and the in vitro apatite forming ability of the synthesized material. The results of this study indicated the successful sol–gel synthesis of an experimental dental ceramic containing low amount of bioactive glass that presented similar structural and morphological characteristics with a commercial feldspathic dental ceramic, while exhibiting in vitro bioactivity. The apatite forming ability of the experimental sol–gel derived feldspathic dental ceramic may trigger the appropriate cellular mechanisms towards the establishment of attachment with the surrounding connective tissue. This attachment could provide a barrier to oral bacteria penetration, prolonging the life expectation of the restorations. - Highlights: • Synthesis of a bioactive sol–gel dental ceramic for fixed prosthetic restorations. • The sol–gel technique promoted the crystallization of

  4. Bioactive glasses: Frontiers and challenges

    Directory of Open Access Journals (Sweden)

    Larry L. Hench

    2015-11-01

    Full Text Available Bioactive glasses were discovered in 1969 and provided for the first time an alternative to nearly inert implant materials. Bioglass formed a rapid, strong and stable bond with host tissues. This article examines the frontiers of research crossed to achieve clinical use of bioactive glasses and glass-ceramics. In the 1980’s it was discovered that bioactive glasses could be used in particulate form to stimulate osteogenesis, which thereby led to the concept of regeneration of tissues. Later, it was discovered that the dissolution ions from the glasses behaved like growth factors, providing signals to the cells. This article summarizes the frontiers of knowledge crossed during four eras of development of bioactive glasses that have led from concept of bioactivity to widespread clinical and commercial use, with emphasis on the first composition, 45S5 Bioglass®. The four eras are: a discovery; b clinical application; c tissue regeneration; and d innovation. Questions still to be answered for the fourth era are included to stimulate innovation in the field and exploration of new frontiers that can be the basis for a general theory of bioactive stimulation of regeneration of tissues and application to numerous clinical needs.

  5. Recent advances on bioactivities of black rice.

    Science.gov (United States)

    Dias, Aécio L de S; Pachikian, Barbara; Larondelle, Yvan; Quetin-Leclercq, Joëlle

    2017-11-01

    Black rice has been consumed for centuries in Asian countries such as China, Korea or Japan. Nowadays, extracts and derivatives are considered as beneficial functional foods because of their high content in several bioactive molecules such as anthocyanins, other phenolics and terpenoids. The purpose of this review is to summarize and discuss recent developments on black rice bioactivities. Some sterols and triterpenoids with potential anticancer properties already tested in vitro and in vivo have been isolated and identified from bran extracts of black rice. Protection against osteoporosis has been suggested for the first time for black rice extracts. Because of its antioxidant and anti-inflammatory properties, black rice also protects liver and kidney from injuries. One clinical study reported the interest of black rice in case of alcohol withdrawal. Several advances have been recently achieved on the understanding of the potential biological effects of black rice and its derivatives. They further confirm that black rice should be considered as a promising source of health-promoting functional foods targeting a large set of noninfectious diseases. However, more clinical studies are needed to support the findings highlighted in this review.

  6. Syntheses of F-18 Labeled Fluoroalkyltyrosine Derivatives

    Energy Technology Data Exchange (ETDEWEB)

    Moon, Byung Seok; Lee, Kyo Chul; Yang, Seung Dae; Chun, Kwon Soo [Korea Institute of Radiological and Medical Sciences, Seoul (Korea, Republic of); Chi, Dae Yoon [Inha Univ., Inchon (Korea, Republic of)

    2005-07-01

    of FET. Herein, we wish to report the synthesis and biological evaluation of four novel nonnatural fluorine-substituted tyrosine derivatives for brain tumor imaging, 3-(2- [{sup 18}F]fluoroethyl)tyrosine 1 (ortho-FET), 3-(3- [{sup 18}F]fluoropropyl)tyrosine 2 (ortho-FPT), O-methyl[3- (2-[{sup 18}F]fluoroethyl)tyrosine 3 (MFET), and Omethyl[ 3-(3-[{sup 18}F]fluoropropyl)tyrosine 4 (MFPT)

  7. Syntheses of F-18 Labeled Fluoroalkyltyrosine Derivatives

    International Nuclear Information System (INIS)

    Moon, Byung Seok; Lee, Kyo Chul; Yang, Seung Dae; Chun, Kwon Soo; Chi, Dae Yoon

    2005-01-01

    to report the synthesis and biological evaluation of four novel nonnatural fluorine-substituted tyrosine derivatives for brain tumor imaging, 3-(2- [ 18 F]fluoroethyl)tyrosine 1 (ortho-FET), 3-(3- [ 18 F]fluoropropyl)tyrosine 2 (ortho-FPT), O-methyl[3- (2-[ 18 F]fluoroethyl)tyrosine 3 (MFET), and Omethyl[ 3-(3-[ 18 F]fluoropropyl)tyrosine 4 (MFPT)

  8. Immense essence of excellence: marine microbial bioactive compounds.

    Science.gov (United States)

    Bhatnagar, Ira; Kim, Se-Kwon

    2010-10-15

    Oceans have borne most of the biological activities on our planet. A number of biologically active compounds with varying degrees of action, such as anti-tumor, anti-cancer, anti-microtubule, anti-proliferative, cytotoxic, photo protective, as well as antibiotic and antifouling properties, have been isolated to date from marine sources. The marine environment also represents a largely unexplored source for isolation of new microbes (bacteria, fungi, actinomycetes, microalgae-cyanobacteria and diatoms) that are potent producers of bioactive secondary metabolites. Extensive research has been done to unveil the bioactive potential of marine microbes (free living and symbiotic) and the results are amazingly diverse and productive. Some of these bioactive secondary metabolites of microbial origin with strong antibacterial and antifungal activities are being intensely used as antibiotics and may be effective against infectious diseases such as HIV, conditions of multiple bacterial infections (penicillin, cephalosporines, streptomycin, and vancomycin) or neuropsychiatric sequelae. Research is also being conducted on the general aspects of biophysical and biochemical properties, chemical structures and biotechnological applications of the bioactive substances derived from marine microorganisms, and their potential use as cosmeceuticals and nutraceuticals. This review is an attempt to consolidate the latest studies and critical research in this field, and to showcase the immense competence of marine microbial flora as bioactive metabolite producers. In addition, the present review addresses some effective and novel approaches of procuring marine microbial compounds utilizing the latest screening strategies of drug discovery.

  9. Immense Essence of Excellence: Marine Microbial Bioactive Compounds

    Directory of Open Access Journals (Sweden)

    Ira Bhatnagar

    2010-10-01

    Full Text Available Oceans have borne most of the biological activities on our planet. A number of biologically active compounds with varying degrees of action, such as anti-tumor, anti-cancer, anti-microtubule, anti-proliferative, cytotoxic, photo protective, as well as antibiotic and antifouling properties, have been isolated to date from marine sources. The marine environment also represents a largely unexplored source for isolation of new microbes (bacteria, fungi, actinomycetes, microalgae-cyanobacteria and diatoms that are potent producers of bioactive secondary metabolites. Extensive research has been done to unveil the bioactive potential of marine microbes (free living and symbiotic and the results are amazingly diverse and productive. Some of these bioactive secondary metabolites of microbial origin with strong antibacterial and antifungal activities are being intensely used as antibiotics and may be effective against infectious diseases such as HIV, conditions of multiple bacterial infections (penicillin, cephalosporines, streptomycin, and vancomycin or neuropsychiatric sequelae. Research is also being conducted on the general aspects of biophysical and biochemical properties, chemical structures and biotechnological applications of the bioactive substances derived from marine microorganisms, and their potential use as cosmeceuticals and nutraceuticals. This review is an attempt to consolidate the latest studies and critical research in this field, and to showcase the immense competence of marine microbial flora as bioactive metabolite producers. In addition, the present review addresses some effective and novel approaches of procuring marine microbial compounds utilizing the latest screening strategies of drug discovery.

  10. Littoral lichens as a novel source of potentially bioactive Actinobacteria.

    Science.gov (United States)

    Parrot, Delphine; Antony-Babu, Sanjay; Intertaglia, Laurent; Grube, Martin; Tomasi, Sophie; Suzuki, Marcelino T

    2015-10-30

    Cultivable Actinobacteria are the largest source of microbially derived bioactive molecules. The high demand for novel antibiotics highlights the need for exploring novel sources of these bacteria. Microbial symbioses with sessile macro-organisms, known to contain bioactive compounds likely of bacterial origin, represent an interesting and underexplored source of Actinobacteria. We studied the diversity and potential for bioactive-metabolite production of Actinobacteria associated with two marine lichens (Lichina confinis and L. pygmaea; from intertidal and subtidal zones) and one littoral lichen (Roccella fuciformis; from supratidal zone) from the Brittany coast (France), as well as the terrestrial lichen Collema auriforme (from a riparian zone, Austria). A total of 247 bacterial strains were isolated using two selective media. Isolates were identified and clustered into 101 OTUs (98% identity) including 51 actinobacterial OTUs. The actinobacterial families observed were: Brevibacteriaceae, Cellulomonadaceae, Gordoniaceae, Micrococcaceae, Mycobacteriaceae, Nocardioidaceae, Promicromonosporaceae, Pseudonocardiaceae, Sanguibacteraceae and Streptomycetaceae. Interestingly, the diversity was most influenced by the selective media rather than lichen species or the level of lichen thallus association. The potential for bioactive-metabolite biosynthesis of the isolates was confirmed by screening genes coding for polyketide synthases types I and II. These results show that littoral lichens are a source of diverse potentially bioactive Actinobacteria.

  11. Bioactive composite for keratoprosthesis skirt.

    Science.gov (United States)

    Laattala, Kaisa; Huhtinen, Reeta; Puska, Mervi; Arstila, Hanna; Hupa, Leena; Kellomäki, Minna; Vallittu, Pekka K

    2011-11-01

    In this study, the fabrication and properties of a synthetic keratoprosthesis skirt for use in osteo-odonto-keratoprosthesis (OOKP) surgery are discussed. In the search for a new material concept, bioactive glass and polymethyl methacrylate (PMMA)-based composites were prepared. Three different bioactive glasses (i.e. 45S5, S53P4 and 1-98) and one slowly resorbing glass, FL107, with two different forms (i.e. particles and porous glass structures) were employed in the fabrication of specimens. In in vitro studies, the dissolution behaviour in simulated aqueous humour, compressive properties, and pore formation of the composites were investigated. According to the results, FL107 dissolved very slowly (2.4% of the initial glass content in three weeks); thus, the pore formation of the FL107 composite was also observed to be restricted. The dissolution rates of the bioactive glass-PMMA composites were greater (12%-17%). These faster dissolving bioactive glass particles caused some porosity on the outermost surfaces of the composite. The slight surface porosity was also confirmed by a decrease in compressive properties. During six weeks' in vitro dissolution, the compressive strength of the test specimens containing particles decreased by 22% compared to values in dry conditions (90-107 MPa). These results indicate that the bioactive composites could be stable synthetic candidates for a keratoprosthesis skirt in the treatment of severely damaged or diseased cornea. Copyright © 2011 Elsevier Ltd. All rights reserved.

  12. Synthesis and in vitro bioactivity of mesoporous bioactive glass scaffolds

    Energy Technology Data Exchange (ETDEWEB)

    Shih, C.J., E-mail: cjshih@kmu.edu.tw [Department of Fragrance and Cosmetic Science, College of Pharmacy, Kaohsiung Medical University, Kaohsiung 807, Taiwan (China); Chen, H.T. [Department of Fragrance and Cosmetic Science, College of Pharmacy, Kaohsiung Medical University, Kaohsiung 807, Taiwan (China); Huang, L.F. [School of Pharmacy, College of Pharmacy, Kaohsiung Medical University, Kaohsiung 807, Taiwan (China); Lu, P.S.; Chang, H.F. [Department of Fragrance and Cosmetic Science, College of Pharmacy, Kaohsiung Medical University, Kaohsiung 807, Taiwan (China); Chang, I.L., E-mail: 84004@cch.org.tw [Department of Orthopaedic Surgery, Chang-Hua Christian Hospital, Changhua 500, Taiwan (China)

    2010-06-15

    The main objective of the present study was to determine the effect of thermal treatment procedures (calcination temperature, heating rate and duration time) on the synthesis of SiO{sub 2}-CaO-P{sub 2}O{sub 5} mesoporous bioactive glass scaffolds. This is accomplished by thermogravimetric analyses, Fourier transform infrared (FTIR) absorption spectra, X-ray diffraction (XRD) and by analysis of nitrogen adsorption/desorption isotherms. In vitro bioactivity can also be assessed by the cytotoxic effect of the glasses on the NIH-3T3 cell line, and by characterization of MC-3T3-E1 cell attachment.

  13. Synthesis and in vitro bioactivity of mesoporous bioactive glass scaffolds

    International Nuclear Information System (INIS)

    Shih, C.J.; Chen, H.T.; Huang, L.F.; Lu, P.S.; Chang, H.F.; Chang, I.L.

    2010-01-01

    The main objective of the present study was to determine the effect of thermal treatment procedures (calcination temperature, heating rate and duration time) on the synthesis of SiO 2 -CaO-P 2 O 5 mesoporous bioactive glass scaffolds. This is accomplished by thermogravimetric analyses, Fourier transform infrared (FTIR) absorption spectra, X-ray diffraction (XRD) and by analysis of nitrogen adsorption/desorption isotherms. In vitro bioactivity can also be assessed by the cytotoxic effect of the glasses on the NIH-3T3 cell line, and by characterization of MC-3T3-E1 cell attachment.

  14. Microbial production of natural and non-natural flavonoids: Pathway engineering, directed evolution and systems/synthetic biology.

    Science.gov (United States)

    Pandey, Ramesh Prasad; Parajuli, Prakash; Koffas, Mattheos A G; Sohng, Jae Kyung

    2016-01-01

    In this review, we address recent advances made in pathway engineering, directed evolution, and systems/synthetic biology approaches employed in the production and modification of flavonoids from microbial cells. The review is divided into two major parts. In the first, various metabolic engineering and system/synthetic biology approaches used for production of flavonoids and derivatives are discussed broadly. All the manipulations/engineering accomplished on the microorganisms since 2000 are described in detail along with the biosynthetic pathway enzymes, their sources, structures of the compounds, and yield of each product. In the second part of the review, post-modifications of flavonoids by four major reactions, namely glycosylations, methylations, hydroxylations and prenylations using recombinant strains are described. Copyright © 2016 Elsevier Inc. All rights reserved.

  15. Bioactive Glass and Glass-Ceramic Scaffolds for Bone Tissue Engineering

    Directory of Open Access Journals (Sweden)

    Aldo R. Boccaccini

    2010-07-01

    Full Text Available Traditionally, bioactive glasses have been used to fill and restore bone defects. More recently, this category of biomaterials has become an emerging research field for bone tissue engineering applications. Here, we review and discuss current knowledge on porous bone tissue engineering scaffolds on the basis of melt-derived bioactive silicate glass compositions and relevant composite structures. Starting with an excerpt on the history of bioactive glasses, as well as on fundamental requirements for bone tissue engineering scaffolds, a detailed overview on recent developments of bioactive glass and glass-ceramic scaffolds will be given, including a summary of common fabrication methods and a discussion on the microstructural-mechanical properties of scaffolds in relation to human bone (structure-property and structure-function relationship. In addition, ion release effects of bioactive glasses concerning osteogenic and angiogenic responses are addressed. Finally, areas of future research are highlighted in this review.

  16. Marine actinobacteria: an important source of bioactive natural products.

    Science.gov (United States)

    Manivasagan, Panchanathan; Kang, Kyong-Hwa; Sivakumar, Kannan; Li-Chan, Eunice C Y; Oh, Hyun-Myung; Kim, Se-Kwon

    2014-07-01

    Marine environment is largely an untapped source for deriving actinobacteria, having potential to produce novel, bioactive natural products. Actinobacteria are the prolific producers of pharmaceutically active secondary metabolites, accounting for about 70% of the naturally derived compounds that are currently in clinical use. Among the various actinobacterial genera, Actinomadura, Actinoplanes, Amycolatopsis, Marinispora, Micromonospora, Nocardiopsis, Saccharopolyspora, Salinispora, Streptomyces and Verrucosispora are the major potential producers of commercially important bioactive natural products. In this respect, Streptomyces ranks first with a large number of bioactive natural products. Marine actinobacteria are unique enhancing quite different biological properties including antimicrobial, anticancer, antiviral, insecticidal and enzyme inhibitory activities. They have attracted global in the last ten years for their ability to produce pharmaceutically active compounds. In this review, we have focused attention on the bioactive natural products isolated from marine actinobacteria, possessing unique chemical structures that may form the basis for synthesis of novel drugs that could be used to combat resistant pathogenic microorganisms. Copyright © 2014 Elsevier B.V. All rights reserved.

  17. Bioactivity of Minor Milk Components

    DEFF Research Database (Denmark)

    Nguyen, Duc Ninh

    . In particular, 3-15% of very low birth weight preterm infants suffer from the most servere form of intestinal inflammation, known as necrotizing enterocolitis (NEC). This disease is incurable with a high mortality rate of 15-30%. Mother’s breast milk consists of different bioactive constituents...... of infant formula. Thereafter, bioactive milk components which were preserved in gently-processed infant formula were selected for further investigation of their immunomodulatory activity in cell and preterm pig models. We hope this project will contribute to the research on the development of new...

  18. An active site mutant of Escherichia coli cyclopropane fatty acid synthase forms new non-natural fatty acids providing insights on the mechanism of the enzymatic reaction.

    Science.gov (United States)

    E, Guangqi; Drujon, Thierry; Correia, Isabelle; Ploux, Olivier; Guianvarc'h, Dominique

    2013-12-01

    We have produced and purified an active site mutant of the Escherichia coli cyclopropane fatty acid synthase (CFAS) by replacing the strictly conserved G236 within cyclopropane synthases, by a glutamate residue, which corresponds to E146 of the homologous mycolic acid methyltransferase, Hma, producing hydroxymethyl mycolic acids. The G236E CFAS mutant had less than 1% of the in vitro activity of the wild type enzyme. We expressed the G236E CFAS mutant in an E. coli (DE3) strain in which the chromosomal cfa gene had been deleted. After extraction of phospholipids and conversion into the corresponding fatty acid methyl esters (FAMEs), we observed the formation of cyclopropanated FAMEs suggesting that the mutant retained some of the normal activity in vivo. However, we also observed the formation of new C17 methyl-branched unsaturated FAMEs whose structures were determined using GC/MS and NMR analyses. The double bond was located at different positions 8, 9 or 10, and the methyl group at position 10 or 9. Thus, this new FAMEs are likely arising from a 16:1 acyl chain of a phospholipid that had been transformed by the G236E CFAS mutant in vivo. The reaction catalyzed by this G236E CFAS mutant thus starts by the methylation of the unsaturated acyl chain at position 10 or 9 yielding a carbocation at position 9 or 10 respectively. It follows then two competing steps, a normal cyclopropanation or hydride shift/elimination events giving different combinations of alkenes. This study not only provides further evidence that cyclopropane synthases (CSs) form a carbocationic intermediate but also opens the way to CSs engineering for the synthesis of non-natural fatty acids. Copyright © 2013 Elsevier Masson SAS. All rights reserved.

  19. Bioactive glasses potential biomaterials for future therapy

    CERN Document Server

    Kaur, Gurbinder

    2017-01-01

    This book describes the history, origin and basic characteristics of bioactive materials. It includes a chapter dedicated to hydroxyapatite mineral, its formation and its bioactive properties. The authors address how cytotoxicity is a determining step for bioactivity. Applications of bioactive materials in the contexts of tissue regeneration, bone regeneration and cancer therapy are also covered. Silicate, metallic and mesoporous glasses are described, as well as the challenges and future prospects of research in this field.

  20. Quenched/unquenched nano bioactive glass-ceramics: Synthesis and in vitro bioactivity evaluation in Ringer’s solution with BSA

    Directory of Open Access Journals (Sweden)

    Nabian Nima

    2013-01-01

    Full Text Available The paper reports the first attempt at changing cooling treatment of synthesizing method in order to investigate its effect on the physical properties of sol-gel derived nano bioactive glass-ceramic in the system 58SiO2-33CaO-9P2O5 (wt.%. We hypothesized that the method of cooling may affect the properties of nano bioactive glass-ceramic. To test this hypothesis, two different method of cooling treatment was applied after calcinations in synthesizing method. Both quenched and unquenched nano bioactive glass-ceramics were soaked in Ringer’s solution with bovine serum albumin (BSA for bioactivity evaluation. The obtained samples were analyzed for their composition, crystalinity and morphology through X-ray powder diffraction (XRD, Fourier transform infrared spectroscopy (FTIR, surface electron microscope (SEM and transmission electron microscope (TEM. The SEM images showed that the morphology of nano bioactive glass-ceramics was completely changed by quenching process. Results of in vitro bioactivity evaluation revealed that the unquenched attains faster apatite formation ability than the quenched sample. Other properties of these two morphologically different nano bioactive glass-ceramics were strongly discussed.

  1. Bio-actives and Drug

    Indian Academy of Sciences (India)

    Bio-actives. have an effect on or elicit a response from living tissue. Refer to a substance that can be acted upon by a living organism or by an extract from a living organism. are constituents in foods or dietary supplements, other than those needed to meet basic nutritional needs, that are responsible for changes in health ...

  2. The influence of precursor addition order on the porosity of sol-gel bioactive glasses.

    Science.gov (United States)

    Fernando, Delihta; Colon, Pierre; Cresswell, Mark; Journet, Catherine; Pradelle-Plasse, Nelly; Jackson, Phil; Grosgogeat, Brigitte; Attik, Nina

    2018-06-16

    The superior textural properties of sol-gel derived bioactive glasses compared to conventional melt quench glasses accounts for their accelerated bioactivity in vitro. Several studies have explored ways to improve the surface properties of sol-gel glasses in order to maximise their efficiency for bone and tooth regeneration. In this study, we investigated the effect of order of network modifying precursor addition on the textural properties of sol-gel derived bioactive glasses. The effect of precursor addition order on the glass characteristics was assessed by switching the order of network modifying precursor (calcium acetate monohydrate and sodium acetate anhydrous) addition for a fixed composition of bioactive glass (75SiO 2 :5CaO:10Na 2 O:10P 2 O 5 ). The results of this study showed that the order of precursor addition does influence the porosity of these glasses. For the glasses of a fixed composition and preparation conditions we achieved a doubling of surface area, a 1.5 times increase in pore volume and a 1.2 times decrease in pore size just by the mixing the network modifying precursors and adding them together in the sol-gel preparation. This simple and straightforward route adaptation to the preparation of bioactive glasses would allow us to enhance the textural properties of existing and novel composition of bioactive glasses and thus accelerate their bioactivity. Copyright © 2018 The Academy of Dental Materials. Published by Elsevier Inc. All rights reserved.

  3. Bioactive Triterpenes from the Fungus Piptoporus betulinus

    Directory of Open Access Journals (Sweden)

    Zeyad Alresly

    2016-01-01

    Full Text Available Phytochemical investigation of the ethyl acetate extract of the fruiting bodies from the basidiomycete Piptoporus betulinus led to the isolation of a new bioactive lanostane triterpene identified as 3 b -acetoxy-16-hydroxy-24-oxo-5α-lanosta-8- ene-21-oic acid (1. In addition, ten known triterpenes, polyporenic acid A (5, polyporenic acid C (4, three derivatives of polyporenic acid A (8, 10, 11, betulinic acid (3, betulin (2, ergosterol peroxide (6, 9,11-dehydroergosterol peroxide (7, and fomefficinic acid (9, were also isolated from the fungus. All isolated compounds were tested for antimicrobial activity against some Gram-positive and Gram-negative bacteria as well as against a fungal strain. The new triterpene and some of the other compounds showed antimicrobial activity against Gram-positive bacteria.

  4. ITPI: Initial Transcription Process-Based Identification Method of Bioactive Components in Traditional Chinese Medicine Formula

    Directory of Open Access Journals (Sweden)

    Baixia Zhang

    2016-01-01

    Full Text Available Identification of bioactive components is an important area of research in traditional Chinese medicine (TCM formula. The reported identification methods only consider the interaction between the components and the target proteins, which is not sufficient to explain the influence of TCM on the gene expression. Here, we propose the Initial Transcription Process-based Identification (ITPI method for the discovery of bioactive components that influence transcription factors (TFs. In this method, genome-wide chip detection technology was used to identify differentially expressed genes (DEGs. The TFs of DEGs were derived from GeneCards. The components influencing the TFs were derived from STITCH. The bioactive components in the formula were identified by evaluating the molecular similarity between the components in formula and the components that influence the TF of DEGs. Using the formula of Tian-Zhu-San (TZS as an example, the reliability and limitation of ITPI were examined and 16 bioactive components that influence TFs were identified.

  5. Structural basis for the site-specific incorporation of lysine derivatives into proteins.

    Directory of Open Access Journals (Sweden)

    Veronika Flügel

    Full Text Available Posttranslational modifications (PTMs of proteins determine their structure-function relationships, interaction partners, as well as their fate in the cell and are crucial for many cellular key processes. For instance chromatin structure and hence gene expression is epigenetically regulated by acetylation or methylation of lysine residues in histones, a phenomenon known as the 'histone code'. Recently it was shown that these lysine residues can furthermore be malonylated, succinylated, butyrylated, propionylated and crotonylated, resulting in significant alteration of gene expression patterns. However the functional implications of these PTMs, which only differ marginally in their chemical structure, is not yet understood. Therefore generation of proteins containing these modified amino acids site specifically is an important tool. In the last decade methods for the translational incorporation of non-natural amino acids using orthogonal aminoacyl-tRNA synthetase (aaRS:tRNAaaCUA pairs were developed. A number of studies show that aaRS can be evolved to use non-natural amino acids and expand the genetic code. Nevertheless the wild type pyrrolysyl-tRNA synthetase (PylRS from Methanosarcina mazei readily accepts a number of lysine derivatives as substrates. This enzyme can further be engineered by mutagenesis to utilize a range of non-natural amino acids. Here we present structural data on the wild type enzyme in complex with adenylated ε-N-alkynyl-, ε-N-butyryl-, ε-N-crotonyl- and ε-N-propionyl-lysine providing insights into the plasticity of the PylRS active site. This shows that given certain key features in the non-natural amino acid to be incorporated, directed evolution of this enzyme is not necessary for substrate tolerance.

  6. Systematic Environmental Impact Assessment for Non-natural Reserve Areas: A Case Study of the Chaishitan Water Conservancy Project on Land Use and Plant Diversity in Yunnan, China

    Directory of Open Access Journals (Sweden)

    Zhi-Xin Zhu

    2017-06-01

    Full Text Available Environmental impact assessment (EIA before and after the establishment of a Water Conservancy Project (WCP is of great theoretical and practical importance for assessing the effectiveness of ecological restoration efforts. WCPs rehabilitate flood-damaged areas or other regions hit by disasters by controlling and redistributing surface water and groundwater. Using Geographic Information System (GIS and Composite Evaluation Index (CEI in predictive modeling, we studied the degree to which a WCP could change land use, plant communities, and species diversity in Yunnan, China. Via modeling, we quantified likely landscape pattern changes and linked them to naturality (i.e., the percentage of secondary vegetation types, diversity, and stability together with the human interferences (e.g., conservation or restoration project of an ecosystem. The value of each index was determined by the evaluation system, and the weight percentage was decided through Analytical Hierarchy Process (AHP. We found that minor land-use changes would occur after the Chaishitan WCP was theoretically established. The greatest decline was farmland (0.079%, followed by forest (0.066%, with the least decline in water bodies (0.020%. We found 1,076 vascular plant species (including subspecies, varieties and form belonging to 165 families and 647 genera in Chaishitan irrigation area before the water conservancy establishment. The naturality and diversity decreased 11.18 and 10.16% respectively. The CEI was 0.92, which indicated that Chaishitan WCP will enhance local landscape heterogeneity, and it will not deteriorate local ecological quality. Our study proposes a comprehensive ecological evaluation system for this WCP and further suggests the importance of including the ecological and environmental consequences of the WCP, along with the well-established socioeconomic evaluation systems for non-natural reserve areas. We conclude that the Chaishitan WCP will have minor

  7. Enhancing bioactive peptide release and identification using targeted enzymatic hydrolysis of milk proteins.

    Science.gov (United States)

    Nongonierma, Alice B; FitzGerald, Richard J

    2018-06-01

    Milk proteins have been extensively studied for their ability to yield a range of bioactive peptides following enzymatic hydrolysis/digestion. However, many hurdles still exist regarding the widespread utilization of milk protein-derived bioactive peptides as health enhancing agents for humans. These mostly arise from the fact that most milk protein-derived bioactive peptides are not highly potent. In addition, they may be degraded during gastrointestinal digestion and/or have a low intestinal permeability. The targeted release of bioactive peptides during the enzymatic hydrolysis of milk proteins may allow the generation of particularly potent bioactive hydrolysates and peptides. Therefore, the development of milk protein hydrolysates capable of improving human health requires, in the first instance, optimized targeted release of specific bioactive peptides. The targeted hydrolysis of milk proteins has been aided by a range of in silico tools. These include peptide cutters and predictive modeling linking bioactivity to peptide structure [i.e., molecular docking, quantitative structure activity relationship (QSAR)], or hydrolysis parameters [design of experiments (DOE)]. Different targeted enzymatic release strategies employed during the generation of milk protein hydrolysates are reviewed herein and their limitations are outlined. In addition, specific examples are provided to demonstrate how in silico tools may help in the identification and discovery of potent milk protein-derived peptides. It is anticipated that the development of novel strategies employing a range of in silico tools may help in the generation of milk protein hydrolysates containing potent and bioavailable peptides, which in turn may be used to validate their health promoting effects in humans. Graphical abstract The targeted enzymatic hydrolysis of milk proteins may allow the generation of highly potent and bioavailable bioactive peptides.

  8. Bioactive peptides released from in vitro digestion of human milk with or without pasteurization.

    Science.gov (United States)

    Wada, Yasuaki; Lönnerdal, Bo

    2015-04-01

    Pasteurized donor human milk (HM) serves as the best alternative for breast-feeding when availability of mother's milk is limited. Pasteurization is also applied to mother's own milk for very low birth weight infants, who are vulnerable to microbial infection. Whether pasteurization affects protein digestibility and therefore modulates the profile of bioactive peptides released from HM proteins by gastrointestinal digestion, has not been examined to date. HM with and without pasteurization (62.5 °C for 30 min) were subjected to in vitro gastrointestinal digestion, followed by peptidomic analysis to compare the formation of bioactive peptides. Some of the bioactive peptides, such as caseinophosphopeptide homologues, a possible opioid peptide (or propeptide), and an antibacterial peptide, were present in undigested HM and showed resistance to in vitro digestion, suggesting that these peptides are likely to exert their bioactivities in the gastrointestinal lumen, or be stably transported to target organs. In vitro digestion of HM released a large variety of bioactive peptides such as angiotensin I-converting enzyme-inhibitory, antioxidative, and immunomodulatory peptides. Bioactive peptides were released largely in the same manner with and without pasteurization. Provision of pasteurized HM may be as beneficial as breast-feeding in terms of milk protein-derived bioactive peptides.

  9. Hierarchical Structures and Shaped Particles of Bioactive Glass and Its In Vitro Bioactivity

    Directory of Open Access Journals (Sweden)

    U. Boonyang

    2013-01-01

    Full Text Available In this study, bioactive glass particles with controllable structure and porosity were prepared using dual-templating methods. Block copolymers used as one template component produced mesopores in the calcined samples. Polymer colloidal crystals as the other template component yielded either three-dimensionally ordered macroporous (3DOM products or shaped bioactive glass nanoparticles. The in vitro bioactivity of these bioactive glasses was studied by soaking the samples in simulated body fluid (SBF at body temperature (37°C for varying lengths of time and monitoring the formation of bone-like apatite on the surface of the bioactive glass. A considerable bioactivity was found that all of bioactive glass samples have the ability to induce the formation of an apatite layer on its surface when in contact with SBF. The development of bone-like apatite is faster for 3DOM bioactive glasses than for nanoparticles.

  10. Enhanced Antifungal Bioactivity of Coptis Rhizome Prepared by Ultrafining Technology

    Directory of Open Access Journals (Sweden)

    Ping-Chung Kuo

    2014-01-01

    Full Text Available The aim of this study was to identify and quantify the bioactive constituents in the methanol extracts of Coptis Rhizome prepared by ultrafining technology. The indicator compound was identified by spectroscopic method and its purity was determined by HPLC. Moreover, the crude extracts and indicator compound were examined for their ability to inhibit the growth of Rhizoctonia solani Kühn AG-4 on potato dextrose agar plates. The indicator compound is a potential candidate as a new plant derived pesticide to control Rhizoctonia damping-off in vegetable seedlings. In addition, the extracts of Coptis Rhizome prepared by ultrafining technology displayed higher contents of indicator compound; they not only improve their bioactivity but also reduce the amount of the pharmaceuticals required and, thereby, decrease the environmental degradation associated with the harvesting of the raw products.

  11. Bioactive glasses materials, properties and applications

    CERN Document Server

    Ylänen, Heimo

    2011-01-01

    Due to their biocompatibility and bioactivity, bioactive glasses are used as highly effective implant materials throughout the human body to replace or repair damaged tissue. As a result, they have been in continuous use since shortly after their invention in the late 1960s and are the subject of extensive research worldwide.Bioactive glasses provides readers with a detailed review of the current status of this unique material, its properties, technologies and applications. Chapters in part one deal with the materials and mechanical properties of bioactive glass, examining topics such

  12. Bioactive content, hepatoprotective and antioxidant activities of ...

    African Journals Online (AJOL)

    Bioactive content, hepatoprotective and antioxidant activities of whole plant extract of Micromeria fruticosa (L) Druce ssp Serpyllifolia F Lamiaceae against Carbon tetrachloride-induced hepatotoxicity in mice.

  13. Bioactivity evolution of the surface functionalized bioactive glasses.

    Science.gov (United States)

    Magyari, Klára; Baia, Lucian; Vulpoi, Adriana; Simon, Simion; Popescu, Octavian; Simon, Viorica

    2015-02-01

    The formation of a calcium phosphate layer on the surface of the SiO2 -CaO-P2 O5 glasses after immersion in simulated body fluid (SBF) generally demonstrates the bioactivity of these materials. Grafting of the surface by chemical bonding can minimize the structural changes in protein adsorbed on the surface. Therefore, in this study our interest was to evaluate the bioactivity and blood biocompatibility of the SiO2 -CaO-P2 O5 glasses after their surface modification by functionalization with aminopropyl-triethoxysilane and/or by fibrinogen. It is shown that the fibrinogen adsorbed on the glass surfaces induces a growing of the apatite-like layer. It is also evidenced that the protein content from SBF influences the growth of the apatite-like layer. Furthermore, the good blood compatibility of the materials after fibrinogen and bovine serum albumin adsorption is proved from the assessment of the β-sheet-β-turn ratio. © 2014 Wiley Periodicals, Inc.

  14. Bioactive Components in Fish Venoms

    Science.gov (United States)

    Ziegman, Rebekah; Alewood, Paul

    2015-01-01

    Animal venoms are widely recognized excellent resources for the discovery of novel drug leads and physiological tools. Most are comprised of a large number of components, of which the enzymes, small peptides, and proteins are studied for their important bioactivities. However, in spite of there being over 2000 venomous fish species, piscine venoms have been relatively underrepresented in the literature thus far. Most studies have explored whole or partially fractioned venom, revealing broad pharmacology, which includes cardiovascular, neuromuscular, cytotoxic, inflammatory, and nociceptive activities. Several large proteinaceous toxins, such as stonustoxin, verrucotoxin, and Sp-CTx, have been isolated from scorpaenoid fish. These form pores in cell membranes, resulting in cell death and creating a cascade of reactions that result in many, but not all, of the physiological symptoms observed from envenomation. Additionally, Natterins, a novel family of toxins possessing kininogenase activity have been found in toadfish venom. A variety of smaller protein toxins, as well as a small number of peptides, enzymes, and non-proteinaceous molecules have also been isolated from a range of fish venoms, but most remain poorly characterized. Many other bioactive fish venom components remain to be discovered and investigated. These represent an untapped treasure of potentially useful molecules. PMID:25941767

  15. Bioactive Glasses in Dentistry: A Review

    Directory of Open Access Journals (Sweden)

    Abbasi Z

    2015-03-01

    Full Text Available Bioactive glasses are silicate-based and can form a strong chemical bond with the tissues. These biomaterials are highly biocompatible and can form a hydroxyapatite layer when implanted in the body or soaked in the simulated body fluid. Due to several disadvantages, conventional glass processing method including melting of glass components, is replaced by sol-gel method with a large number of benefits such as low processing temperature, higher purity and homogeneity and therefore better control of bioactivity. Bioactive glasses have a wide range of applications, particularly in dentistry. These glasses can be used as particulates or monolithic shapes and porous or dense constructs in different applications such as remineralization or hypersensitivity treatment. Some properties of bioactive glasses such as antibacterial properties can be promoted by adding different elements into the glass. Bioactive glasses can also be used to modify different biocompatible materials that need to be bioactive. This study reviews the significant developments of bioactive glasses in clinical application, especially dentistry. Furthermore, we will discuss the field of bioactive glasses from beginning to the current developments, which includes processing methods, applications, and properties of these glasses.

  16. Laser cladding of bioactive glass coatings.

    Science.gov (United States)

    Comesaña, R; Quintero, F; Lusquiños, F; Pascual, M J; Boutinguiza, M; Durán, A; Pou, J

    2010-03-01

    Laser cladding by powder injection has been used to produce bioactive glass coatings on titanium alloy (Ti6Al4V) substrates. Bioactive glass compositions alternative to 45S5 Bioglass were demonstrated to exhibit a gradual wetting angle-temperature evolution and therefore a more homogeneous deposition of the coating over the substrate was achieved. Among the different compositions studied, the S520 bioactive glass showed smoother wetting angle-temperature behavior and was successfully used as precursor material to produce bioactive coatings. Coatings processed using a Nd:YAG laser presented calcium silicate crystallization at the surface, with a uniform composition along the coating cross-section, and no significant dilution of the titanium alloy was observed. These coatings maintain similar bioactivity to that of the precursor material as demonstrated by immersion in simulated body fluid. Copyright 2009 Acta Materialia Inc. Published by Elsevier Ltd. All rights reserved.

  17. Therapeutic Properties of Bioactive Compounds from Different Honeybee Products.

    Science.gov (United States)

    Cornara, Laura; Biagi, Marco; Xiao, Jianbo; Burlando, Bruno

    2017-01-01

    Honeybees produce honey, royal jelly, propolis, bee venom, bee pollen, and beeswax, which potentially benefit to humans due to the bioactives in them. Clinical standardization of these products is hindered by chemical variability depending on honeybee and botanical sources, but different molecules have been isolated and pharmacologically characterized. Major honey bioactives include phenolics, methylglyoxal, royal jelly proteins (MRJPs), and oligosaccharides. In royal jelly there are antimicrobial jelleins and royalisin peptides, MRJPs, and hydroxy-decenoic acid derivatives, notably 10-hydroxy-2-decenoic acid (10-HDA), with antimicrobial, anti-inflammatory, immunomodulatory, neuromodulatory, metabolic syndrome preventing, and anti-aging activities. Propolis contains caffeic acid phenethyl ester and artepillin C, specific of Brazilian propolis, with antiviral, immunomodulatory, anti-inflammatory and anticancer effects. Bee venom consists of toxic peptides like pain-inducing melittin, SK channel blocking apamin, and allergenic phospholipase A2. Bee pollen is vitaminic, contains antioxidant and anti-inflammatory plant phenolics, as well as antiatherosclerotic, antidiabetic, and hypoglycemic flavonoids, unsaturated fatty acids, and sterols. Beeswax is widely used in cosmetics and makeup. Given the importance of drug discovery from natural sources, this review is aimed at providing an exhaustive screening of the bioactive compounds detected in honeybee products and of their curative or adverse biological effects.

  18. Therapeutic Properties of Bioactive Compounds from Different Honeybee Products

    Directory of Open Access Journals (Sweden)

    Laura Cornara

    2017-06-01

    Full Text Available Honeybees produce honey, royal jelly, propolis, bee venom, bee pollen, and beeswax, which potentially benefit to humans due to the bioactives in them. Clinical standardization of these products is hindered by chemical variability depending on honeybee and botanical sources, but different molecules have been isolated and pharmacologically characterized. Major honey bioactives include phenolics, methylglyoxal, royal jelly proteins (MRJPs, and oligosaccharides. In royal jelly there are antimicrobial jelleins and royalisin peptides, MRJPs, and hydroxy-decenoic acid derivatives, notably 10-hydroxy-2-decenoic acid (10-HDA, with antimicrobial, anti-inflammatory, immunomodulatory, neuromodulatory, metabolic syndrome preventing, and anti-aging activities. Propolis contains caffeic acid phenethyl ester and artepillin C, specific of Brazilian propolis, with antiviral, immunomodulatory, anti-inflammatory and anticancer effects. Bee venom consists of toxic peptides like pain-inducing melittin, SK channel blocking apamin, and allergenic phospholipase A2. Bee pollen is vitaminic, contains antioxidant and anti-inflammatory plant phenolics, as well as antiatherosclerotic, antidiabetic, and hypoglycemic flavonoids, unsaturated fatty acids, and sterols. Beeswax is widely used in cosmetics and makeup. Given the importance of drug discovery from natural sources, this review is aimed at providing an exhaustive screening of the bioactive compounds detected in honeybee products and of their curative or adverse biological effects.

  19. A sucrose-derived scaffold for multimerization of bioactive peptides.

    Science.gov (United States)

    Rao, Venkataramanarao; Alleti, Ramesh; Xu, Liping; Tafreshi, Narges K; Morse, David L; Gillies, Robert J; Mash, Eugene A

    2011-11-01

    A spherical molecular scaffold bearing eight terminal alkyne groups was synthesized in one step from sucrose. One or more copies of a tetrapeptide azide, either N(3)(CH(2))(5)(CO)-His-DPhe-Arg-Trp-NH(2) (MSH4) or N(3)(CH(2))(5)(CO)-Trp-Met-Asp-Phe-NH(2) (CCK4), were attached to the scaffold via the copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC) reaction. Competitive binding assays using Eu-labeled probes based on the superpotent ligands Ser-Tyr-Ser-Nle-Glu-His-DPhe-Arg-Trp-Gly-Lys-Pro-Val-NH(2) (NDP-α-MSH) and Asp-Tyr-Met-Gly-Trp-Met-Asp-Phe-NH(2) (CCK8) were used to study the interactions of monovalent and multivalent MSH4 and CCK4 constructs with Hek293 cells engineered to overexpress MC4R and CCK2R. All of the monovalent and multivalent MSH4 constructs exhibited binding comparable to that of the parental ligand, suggesting that either the ligand spacing was inappropriate for multivalent binding, or MSH4 is too weak a binder for a second 'anchoring' binding event to occur before the monovalently-bound construct is released from the cell surface. In contrast with this behavior, monovalent CCK4 constructs were significantly less potent than the parental ligand, while multivalent CCK4 constructs were as or more potent than the parental ligand. These results are suggestive of multivalent binding, which may be due to increased residence times for monovalently bound CCK4 constructs on the cell surface relative to MSH4 constructs, the greater residence time being necessary for the establishment of multivalent binding. Copyright © 2011 Elsevier Ltd. All rights reserved.

  20. Syntheses, Crystal Structures and Bioactivities of Two Novel Isatin Derivatives

    Institute of Scientific and Technical Information of China (English)

    SHANG Jian-li; LI Hui-dong; SHANG Jun; SONG Hai-bin; LI Zheng-ming; WANG Jian-guo

    2011-01-01

    Two novel compoundsl-(4-fluorobenzyl)-4-chloro-(Z)-3-benzoylhydrazono-2-indolinone(1) and 1-(4-methoxybenzyl)-(Z)-3-benzoylhydrazono-2-indolinone(2) were synthesized and their crystal structures were determined by single-crystal X-ray diffraction.Compound 1(C22H15ClFN3O2) crystallized in the triclinic system,space group P1- with a=0.94198(19) nm,b=1.4339(3) nm,c=1.5018(3) nm,a=101.58(3)°,β=102.96(3)°,γ=102.73°,V=1.8602(6) nm3,Mr=407.82,Dc=1.456 g/cm3,μ=0.240 mm-1,F(000)=840,Z=4,R1=0.0442 and wR2=0.1064.Compound 2(C23H19N3O3) crystallized in the triclinic system,space group P1- with a=1.0022(2) nm,b=1.0192(2) nm,c=1.0461(2) nm,a=99.86(3)°,β=117.30(3)°,γ=94.13(3)°,V=0.9215(3) nm3,Mr=385.41,Dc=1.389 g/cm3,μ=0.094mm-1,F(000)=404,Z=2,R1=0.0403 and wR2=0.1142.The preliminary herbicidal activities of the two compounds were also evaluated.

  1. Influence of sodium content on the properties of bioactive glasses for use in air abrasion

    International Nuclear Information System (INIS)

    Farooq, Imran; Brauer, Delia S; Hill, Robert G; Tylkowski, Maxi; Müller, Steffen; Janicki, Tomasz

    2013-01-01

    Air abrasion is used in minimally invasive dentistry for preparing cavities, while removing no or little sound dentine or enamel, and the use of bioactive glass (rather than alumina) as an abrasive could aid in tooth remineralization. Melt-derived bioactive glasses (SiO 2 –P 2 O 5 –CaO–CaF 2 –Na 2 O) with low sodium content (0 to 10 mol% Na 2 O in exchange for CaO) for increased hardness, high phosphate content for high bioactivity and fluoride content for release of fluoride and formation of fluorapatite were produced, and particles between 38 and 80 µm in size were used for cutting soda-lime silicate glass microscope slides and human enamel. Vickers hardness increased with decreasing Na 2 O content, owing to a more compact silicate network in low sodium content glasses, resulting in shorter cutting times. Cutting times using bioactive glass were significantly longer than using the alumina control (29 µm) when tested on microscope slides; however, glasses showed more comparable results when cutting human enamel. The bioactive glasses formed apatite in Tris buffer within 6 h, which was significantly faster than Bioglass® 45S5 (24 h), suggesting that the hardness of the glasses makes them suitable for air abrasion application, while their high bioactivity and fluoride content make them of interest for tooth remineralization. (paper)

  2. Influence of sodium content on the properties of bioactive glasses for use in air abrasion.

    Science.gov (United States)

    Farooq, Imran; Tylkowski, Maxi; Müller, Steffen; Janicki, Tomasz; Brauer, Delia S; Hill, Robert G

    2013-12-01

    Air abrasion is used in minimally invasive dentistry for preparing cavities, while removing no or little sound dentine or enamel, and the use of bioactive glass (rather than alumina) as an abrasive could aid in tooth remineralization. Melt-derived bioactive glasses (SiO2-P2O5-CaO-CaF2-Na2O) with low sodium content (0 to 10 mol% Na2O in exchange for CaO) for increased hardness, high phosphate content for high bioactivity and fluoride content for release of fluoride and formation of fluorapatite were produced, and particles between 38 and 80 µm in size were used for cutting soda-lime silicate glass microscope slides and human enamel. Vickers hardness increased with decreasing Na2O content, owing to a more compact silicate network in low sodium content glasses, resulting in shorter cutting times. Cutting times using bioactive glass were significantly longer than using the alumina control (29 µm) when tested on microscope slides; however, glasses showed more comparable results when cutting human enamel. The bioactive glasses formed apatite in Tris buffer within 6 h, which was significantly faster than Bioglass® 45S5 (24 h), suggesting that the hardness of the glasses makes them suitable for air abrasion application, while their high bioactivity and fluoride content make them of interest for tooth remineralization.

  3. Bioactivation of Phytoestrogens: Intestinal Bacteria and Health.

    Science.gov (United States)

    Landete, J M; Arqués, J; Medina, M; Gaya, P; de Las Rivas, B; Muñoz, R

    2016-08-17

    Phytoestrogens are polyphenols similar to human estrogens found in plants or derived from plant precursors. Phytoestrogens are found in high concentration in soya, flaxseed and other seeds, fruits, vegetables, cereals, tea, chocolate, etc. They comprise several classes of chemical compounds (stilbenes, coumestans, isoflavones, ellagitannins, and lignans) which are structurally similar to endogenous estrogens but which can have both estrogenic and antiestrogenic effects. Although epidemiological and experimental evidence indicates that intake of phytoestrogens in foods may be protective against certain chronic diseases, discrepancies have been observed between in vivo and in vitro experiments. The microbial transformations have not been reported so far in stilbenes and coumestans. However, isoflavones, ellagitanins, and lignans are metabolized by intestinal bacteria to produce equol, urolithins, and enterolignans, respectively. Equol, urolithin, and enterolignans are more bioavailable, and have more estrogenic/antiestrogenic and antioxidant activity than their precursors. Moreover, equol, urolithins and enterolignans have anti-inflammatory effects and induce antiproliferative and apoptosis-inducing activities. The transformation of isoflavones, ellagitanins, and lignans by intestinal microbiota is essential to be protective against certain chronic diseases, as cancer, cardiovascular disease, osteoporosis, and menopausal symptoms. Bioavailability, bioactivity, and health effects of dietary phytoestrogens are strongly determined by the intestinal bacteria of each individual.

  4. Chemical Structures and Bioactivities of Sulfated Polysaccharides from Marine Algae

    Directory of Open Access Journals (Sweden)

    H. Stephen Ewart

    2011-02-01

    Full Text Available Sulfated polysaccharides and their lower molecular weight oligosaccharide derivatives from marine macroalgae have been shown to possess a variety of biological activities. The present paper will review the recent progress in research on the structural chemistry and the bioactivities of these marine algal biomaterials. In particular, it will provide an update on the structural chemistry of the major sulfated polysaccharides synthesized by seaweeds including the galactans (e.g., agarans and carrageenans, ulvans, and fucans. It will then review the recent findings on the anticoagulant/antithrombotic, antiviral, immuno-inflammatory, antilipidemic and antioxidant activities of sulfated polysaccharides and their potential for therapeutic application.

  5. Bioactivities by a crude extract from the Greenlandic Pseudomonas sp. In5 involves the nonribosomal peptides, nunamycin and nunapeptin

    DEFF Research Database (Denmark)

    Frydenlund Michelsen, Charlotte; Jensen, Helle; Venditto, Vincent J.

    2015-01-01

    Bioactive microbial metabolites provide a successful source of novel compounds with pharmaceutical potentials. The bacterium Pseudomonas sp. In5 is a biocontrol strain isolated from a plant disease suppressive soil in Greenland, which produces two antimicrobial nonribosomal peptides (NRPs), nunap......), nunapeptin and nunamycin. In this study, we used in vitro antimicrobial and anticancer bioassays to evaluate the potential bioactivities of both a crude extract derived from Pseudomonas sp. In5 and NRPs purified from the crude extract....

  6. Peptides: Production, bioactivity, functionality, and applications

    DEFF Research Database (Denmark)

    Hajfathalian, Mona; Ghelichi, Sakhi; García Moreno, Pedro Jesús

    2017-01-01

    Production of peptides with various effects from proteins of different sources continues to receive academic attention. Researchers of different disciplines are putting increasing efforts to produce bioactive and functional peptides from different sources such as plants, animals, and food industry...... by-products. The aim of this review is to introduce production methods of hydrolysates and peptides and provide a comprehensive overview of their bioactivity in terms of their effects on immune, cardiovascular, nervous, and gastrointestinal systems. Moreover, functional and antioxidant properties...... of hydrolysates and isolated peptides are reviewed. Finally, industrial and commercial applications of bioactive peptides including their use in nutrition and production of pharmaceuticals and nutraceuticals are discussed....

  7. Nutrients and bioactive substances in aquatic organisms

    International Nuclear Information System (INIS)

    Devadasan, K.; Mukundan, M.K.; Antony, P.D.; Viswanathan Nair, P.G.; Perigreen, P.A.; Joseph, Jose

    1994-01-01

    The International Symposium on Nutrients and Bioactive Substances in Aquatic Organisms, was held during 16-17 September 1993 by the Society of Fisheries Technologists (India) to review the progress of research in this area in India and elsewhere. The papers presented indicate that scientific productivity in this field is substantial and that some of the bioactive materials isolated from aquatic organisms have potential application in human health, nutrition and therapy. The symposium focussed attention on toxicants, nutrients and bioactive substances in aquatic organisms in general, and also on pollution of aquatic systems due to thermal effluents. Paper relevant to INIS database is indexed separately. (M.K.V.)

  8. Bioactivities and Health Benefits of Wild Fruits

    Directory of Open Access Journals (Sweden)

    Ya Li

    2016-08-01

    Full Text Available Wild fruits are exotic or underutilized. Wild fruits contain many bioactive compounds, such as anthocyanins and flavonoids. Many studies have shown that wild fruits possess various bioactivities and health benefits, such as free radical scavenging, antioxidant, anti-inflammatory, antimicrobial, and anticancer activity. Therefore, wild fruits have the potential to be developed into functional foods or pharmaceuticals to prevent and treat several chronic diseases. In the present article, we review current knowledge about the bioactivities and health benefits of wild fruits, which is valuable for the exploitation and utilization of wild fruits.

  9. Bioactive Carbohydrates and Peptides in Foods: An Overview of Sources, Downstream Processing Steps and Associated Bioactivities.

    Science.gov (United States)

    Hayes, Maria; Tiwari, Brijesh K

    2015-09-17

    Bioactive peptides and carbohydrates are sourced from a myriad of plant, animal and insects and have huge potential for use as food ingredients and pharmaceuticals. However, downstream processing bottlenecks hinder the potential use of these natural bioactive compounds and add cost to production processes. This review discusses the health benefits and bioactivities associated with peptides and carbohydrates of natural origin and downstream processing methodologies and novel processes which may be used to overcome these.

  10. Synthesis and bioactive evaluations of novel benzotriazole ...

    Indian Academy of Sciences (India)

    Synthesis and bioactive evaluations of novel benzotriazole compounds as ... School of Chemistry and Chemical Engineering, Southwest University, Chongqing 400715, .... −3 mol/L) was prepared by dissolving its solid in doubly distilled water.

  11. Advances on Bioactive Polysaccharides from Medicinal Plants.

    Science.gov (United States)

    Xie, Jian-Hua; Jin, Ming-Liang; Morris, Gordon A; Zha, Xue-Qiang; Chen, Han-Qing; Yi, Yang; Li, Jing-En; Wang, Zhi-Jun; Gao, Jie; Nie, Shao-Ping; Shang, Peng; Xie, Ming-Yong

    2016-07-29

    In recent decades, the polysaccharides from the medicinal plants have attracted a lot of attention due to their significant bioactivities, such as anti-tumor activity, antioxidant activity, anticoagulant activity, antidiabetic activity, radioprotection effect, anti-viral activity, hypolipidemic and immunomodulatory activities, which make them suitable for medicinal applications. Previous studies have also shown that medicinal plant polysaccharides are non-toxic and show no side effects. Based on these encouraging observations, most researches have been focusing on the isolation and identification of polysaccharides, as well as their bioactivities. A large number of bioactive polysaccharides with different structural features and biological effects from medicinal plants have been purified and characterized. This review provides a comprehensive summary of the most recent developments in physiochemical, structural features and biological activities of bioactive polysaccharides from a number of important medicinal plants, such as polysaccharides from Astragalus membranaceus, Dendrobium plants, Bupleurum, Cactus fruits, Acanthopanax senticosus, Angelica sinensis (Oliv.) Diels, Aloe barbadensis Miller, and Dimocarpus longan Lour. Moreover, the paper has also been focused on the applications of bioactive polysaccharides for medicinal applications. Recent studies have provided evidence that polysaccharides from medicinal plants can play a vital role in bioactivities. The contents and data will serve as a useful reference material for further investigation, production, and application of these polysaccharides in functional foods and therapeutic agents.

  12. Polymerization kinetics of experimental bioactive composites containing bioactive glass.

    Science.gov (United States)

    Par, Matej; Tarle, Zrinka; Hickel, Reinhard; Ilie, Nicoleta

    2018-06-21

    To investigate the polymerization kinetics and the degree of conversion (DC) of experimental resin composites with varying amount of bioactive glass 45S5 (BG). Experimental resin composites based on a photo-curable Bis-GMA/TEGDMA resin system were prepared. The composite series contained 0, 5, 10, 20, and 40 wt% of BG and reinforcing fillers up to the total filler amount of 70 wt%. Composite specimens were light cured with 1,219 mW/cm 2 for 20 or 40 s and their DC was monitored during 5 min at the data collection rate of 2 s -1 using attenuated total reflectance Fourier transform infrared spectroscopy (ATR-FTIR). The 5-min DC values for experimental composites were in the range of 42.4-55.9% and 47.3-57.9% for curing times of 20 and 40 s, respectively. The differences in the 5-min DC between curing times of 20 s or 40 s became more pronounced in materials with higher BG amount. Within both curing times, a decreasing trend of the 5-min DC values was observed with the increasing percentage of BG fillers. The maximum polymerization rate also decreased consistently with the increasing BG amount. Unsilanized BG fillers showed a dose-dependent inhibitory effect on polymerization rate and the DC. Extending the curing time from 20 to 40 s showed a limited potential to improve the DC of composites with higher BG amount. The observed inhibitory effect of BG fillers on the polymerization of resin composites may have a negative influence on mechanical properties and biocompatibility. Copyright © 2018. Published by Elsevier Ltd.

  13. Prospects in the use of aptamers for characterizing the structure and stability of bioactive proteins and peptides in food.

    Science.gov (United States)

    Agyei, Dominic; Acquah, Caleb; Tan, Kei Xian; Hii, Hieng Kok; Rajendran, Subin R C K; Udenigwe, Chibuike C; Danquah, Michael K

    2018-01-01

    Food-derived bioactive proteins and peptides have gained acceptance among researchers, food manufacturers and consumers as health-enhancing functional food components that also serve as natural alternatives for disease prevention and/or management. Bioactivity in food proteins and peptides is determined by their conformations and binding characteristics, which in turn depend on their primary and secondary structures. To maintain their bioactivities, the molecular integrity of bioactive peptides must remain intact, and this warrants the study of peptide form and structure, ideally with robust, highly specific and sensitive techniques. Short single-stranded nucleic acids (i.e. aptamers) are known to have high affinity for cognate targets such as proteins and peptides. Aptamers can be produced cost-effectively and chemically derivatized to increase their stability and shelf life. Their improved binding characteristics and minimal modification of the target molecular signature suggests their suitability for real-time detection of conformational changes in both proteins and peptides. This review discusses the developmental progress of systematic evolution of ligands by exponential enrichment (SELEX), an iterative technology for generating cost-effective aptamers with low dissociation constants (K d ) for monitoring the form and structure of bioactive proteins and peptides. The review also presents case studies of this technique in monitoring the structural stability of bioactive peptide formulations to encourage applications in functional foods. The challenges and potential of aptamers in this research field are also discussed. Graphical abstract Advancing bioactive proteins and peptide functionality via aptameric ligands.

  14. Synthesis of N-substituted acetamide derivatives of azinane-bearing ...

    African Journals Online (AJOL)

    The search for new drug candidates with more bioactivity potential is a key research interest in synthetic organic chemistry [1]. The derivatives of heterocyclic compounds have been found to be bioactive, including naturally occurring and synthetically prepared ones [2]. Among these compounds, 1,3,4-oxadiazole derivatives ...

  15. Bioactive peptides: production, health effects and application as natural supplements for functional foods production

    Directory of Open Access Journals (Sweden)

    S. Mirdamadi

    2017-05-01

    Full Text Available Bioactive peptides, are inactive components within the structure of the protein and when they are released by enzymatic hydrolysis, show different physiological functions. Recently, the identification and characterization of bioactive peptides derived from plant and animal sources and different microorganisms is highly regarded. They are produced during enzymatic hydrolysis by gastrointestinal enzymes or enzymes extracted from microorganisms and plants or by proteolytic starter cultures during fermentation process and exhibit different activities including: opioid, mineral binding, immunomodulatory, antioxidant, antimicrobial, anti-inflammatory, chlosterol lowering and so on. Take advantage of bioactive peptides as components of health is related to bio stability assurance, bioavailability and safety of them. The use of computer-based techniques and the use of various databases completed in laboratory studies,  have provided the possibility of studying the mechanisms of action of different peptides.

  16. An overview of the effects of thermal processing on bioactive glasses

    Directory of Open Access Journals (Sweden)

    Bellucci D.

    2010-01-01

    Full Text Available Bioglass® 45S5 is widely used in biomedical applications due to its ability to bond to bone and even to soft tissues. The sintering ability of Bioglass® powders is a key factor from a technological point of view, since its govern the production of advanced devices, ranging from highly porous scaffolds to functionalized coatings. Unfortunately this particular glass composition is prone to crystallize at the temperature required for sintering and this may impair the bioactivity of the original glass. For these reasons, a prerequisite to tailor the fabrication of Bioglass®-derived implants is to understand the interaction between sintering, crystallization and bioactivity. In this work the structural transformations which occur during the heat treatment of Bioglass® are reviewed and a special attention is paid to the sintering and crystallization processes. Moreover the bioactivity of the final glass-ceramics is discussed and some alternative glass formulations are reported.

  17. Role of cellulose functionality in bio-inspired synthesis of nano bioactive glass.

    Science.gov (United States)

    Gupta, Nidhi; Santhiya, Deenan

    2017-06-01

    In search of abundant cheaper natural polymer for bio-inspired bioactive glass nanoparticles synthesis, cellulose and its derivatives have been considered as a template. Different templates explored in the present studies are pure cellulose, methyl cellulose and amine grafted cellulose. To the best of our knowledge, for the first time of the considered templates, pure cellulose and amine grafted cellulose results in in situ nano particulate composite formation while interestingly methyl cellulose proves to be an excellent sacrificial template for the synthesis of uniform bioglass nanoparticles of diameter in the range of 55nm. Further, viscoelastic measurements were carried out using dynamic mechanical analyzer. Herein, an attempt has been made to establish structure-mechanical relationship based on the templates. Moreover, in vitro bioactivity is also observed to be affected by the nature of the template molecule used for the synthesis of bioactive glass. Copyright © 2017 Elsevier B.V. All rights reserved.

  18. Bioactive Compounds of Edible Purple Laver Porphyra sp. (Nori).

    Science.gov (United States)

    Bito, Tomohiro; Teng, Fei; Watanabe, Fumio

    2017-12-13

    Porphyra sp. (nori) is widely cultivated as an important marine crop. Dried nori contains numerous nutrients, including vitamin B 12 , which is the only vitamin absent from plant-derived food sources. Vegetarian diets are low in iron and vitamin B 12 ; depletion of both causes severe anemia. Nori also contains large amounts of iron compared with other plant-derived foods and eicosapentaenoic acid, which is an important fatty acid found in fish oils. In nori, there are also many bioactive compounds that exhibit various pharmacological activities, such as immunomodulation, anticancer, antihyperlipidemic, and antioxidative activities, indicating that consumption of nori is beneficial to human health. However, Porphyra sp. contains toxic metals (arsenic and cadmiun) and/or amphipod allergens, the levels of which vary significantly among nori products. Further evidence from human studies of such beneficial or adverse effects of nori consumption is required.

  19. In vitro bioactivity of polymer matrices reinforced with a bioactive glass phase

    Directory of Open Access Journals (Sweden)

    Oréfice Rodrigo L.

    2000-01-01

    Full Text Available Composites that can mimic the in vitro bioactive behavior of bioactive glasses were designed to fulfill two main features of bioactive glasses that are responsible for their high bond-to-bone rates: (1 capability of providing ions such as calcium and phosphate to the nearby environment and (2 ideal surface structure that allows fast heterogeneous precipitation of hydroxy-carbonate-apatite (HCA. The novel composites were prepared by incorporating bioactive glass particles into polymer matrices. The in vitro bioactivity test was performed by introducing samples into a buffered solution as well as into a simulated body fluid solution. FTIR was used to evaluate the kinetics of HCA (hydroxy-carbonate-apatite precipitation. The results showed that the obtained composites can supply ions, such as silicates and phosphates in rates and concentrations comparable or superior than bulk bioactive glasses. Moreover, the surface chemistry of the composites was altered to mimic the surface of bioactive glasses. It was demonstrated that the in vitro bioactivity of the composites was enhanced by chemically modifying polymer surfaces through the introduction of special alkoxysilane groups.

  20. Dextran hydrogels incorporated with bioactive glass-ceramic: Nanocomposite scaffolds for bone tissue engineering.

    Science.gov (United States)

    Nikpour, Parisa; Salimi-Kenari, Hamed; Fahimipour, Farahnaz; Rabiee, Sayed Mahmood; Imani, Mohammad; Dashtimoghadam, Erfan; Tayebi, Lobat

    2018-06-15

    A series of nanocomposite scaffolds comprised of dextran (Dex) and sol-gel derived bioactive glass ceramic nanoparticles (nBGC: 0-16 (wt%)) were fabricated as bioactive scaffolds for bone tissue engineering. Scanning electron microscopy showed Dex/nBGC scaffolds were consisting of a porous 3D microstructure with an average pore size of 240 μm. Energy-dispersive x-ray spectroscopy illustrated nBGC nanoparticles were homogenously distributed within the Dex matrix at low nBGC content (2 wt%), while agglomeration was observed at higher nBGC contents. It was found that the osmotic pressure and nBGC agglomeration at higher nBGC contents leads to increased water uptake, then reduction of the compressive modulus. Bioactivity of Dex/nBGC scaffolds was validated through apatite formation after submersion in the simulated body fluid. Dex/nBGC composite scaffolds were found to show improved human osteoblasts (HOBs) proliferation and alkaline phosphatase (ALP) activity with increasing nBGC content up to 16 (wt%) over two weeks. Owing to favorable physicochemical and bioactivity properties, the Dex/nBGC composite hydrogels can be offered as promising bioactive scaffolds for bone tissue engineering applications. Copyright © 2018 Elsevier Ltd. All rights reserved.

  1. Bio-active molecules modified surfaces enhanced mesenchymal stem cell adhesion and proliferation

    International Nuclear Information System (INIS)

    Mobasseri, Rezvan; Tian, Lingling; Soleimani, Masoud; Ramakrishna, Seeram; Naderi-Manesh, Hossein

    2017-01-01

    Surface modification of the substrate as a component of in vitro cell culture and tissue engineering, using bio-active molecules including extracellular matrix (ECM) proteins or peptides derived ECM proteins can modulate the surface properties and thereby induce the desired signaling pathways in cells. The aim of this study was to evaluate the behavior of human bone marrow mesenchymal stem cells (hBM-MSCs) on glass substrates modified with fibronectin (Fn), collagen (Coll), RGD peptides (RGD) and designed peptide (R-pept) as bio-active molecules. The glass coverslips were coated with fibronectin, collagen, RGD peptide and R-peptide. Bone marrow mesenchymal stem cells were cultured on different substrates and the adhesion behavior in early incubation times was investigated using scanning electron microscopy (SEM) and confocal microscopy. The MTT assay was performed to evaluate the effect of different bio-active molecules on MSCs proliferation rate during 24 and 72 h. Formation of filopodia and focal adhesion (FA) complexes, two steps of cell adhesion process, were observed in MSCs cultured on bio-active molecules modified coverslips, specifically in Fn coated and R-pept coated groups. SEM image showed well adhesion pattern for MSCs cultured on Fn and R-pept after 2 h incubation, while the shape of cells cultured on Coll and RGD substrates indicated that they might experience stress condition in early hours of culture. Investigation of adhesion behavior, as well as proliferation pattern, suggests R-peptide as a promising bio-active molecule to be used for surface modification of substrate in supporting and inducing cell adhesion and proliferation. - Highlights: • Bioactive molecules modified surface is a strategy to design biomimicry scaffold. • Bi-functional Tat-derived peptide (R-pept) enhanced MSCs adhesion and proliferation. • R-pept showed similar influences to fibronectin on FA formation and attachment.

  2. Microencapsulation of bioactives for food applications.

    Science.gov (United States)

    Dias, Maria Inês; Ferreira, Isabel C F R; Barreiro, Maria Filomena

    2015-04-01

    Health issues are an emerging concern to the world population, and therefore the food industry is searching for novel food products containing health-promoting bioactive compounds, with little or no synthetic ingredients. However, there are some challenges in the development of functional foods, particularly in which the direct use of some bioactives is involved. They can show problems of instability, react with other food matrix ingredients or present strong odour and/or flavours. In this context, microencapsulation emerges as a potential approach to overcome these problems and, additionally, to provide controlled or targeted delivery or release. This work intends to contribute to the field of functional food development by performing a comprehensive review on the microencapsulation methods and materials, the bioactives used (extracts and isolated compounds) and the final application development. Although several studies dealing with microencapsulation of bioactives exist, they are mainly focused on the process development and the majority lack proof of concept for final applications. These factors, together with the lack of regulation, in Europe and in the United States, delay the development of new functional foods and, consequently, their market entry. In conclusion, the potential of microencapsulation to protect bioactive compounds ensuring their bioavailability is shown, but further studies are required, considering both its applicability and incentives by regulatory agencies.

  3. Microbial biotransformation of bioactive flavonoids.

    Science.gov (United States)

    Cao, Hui; Chen, Xiaoqing; Jassbi, Amir Reza; Xiao, Jianbo

    2015-01-01

    The bioactive flavonoids are considered as the most important phytochemicals in food, which exert a wide range of biological benefits for human being. Microbial biotransformation strategies for production of flavonoids have attracted considerable interest because they allow yielding novel flavonoids, which do not exist in nature. In this review, we summarize the existing knowledge on the production and biotransformation of flavonoids by various microbes. The main reactions during microbial biotransformation are hydroxylation, dehydroxylation, O-methylation, O-demethylation, glycosylation, deglycosylation, dehydrogenation, hydrogenation, C ring cleavage of the benzo-γ-pyrone system, cyclization, and carbonyl reduction. Cunninghamella, Penicillium, and Aspergillus strains are very popular to biotransform flavonoids and they can perform almost all the reactions with excellent yields. Aspergillus niger is one of the most applied microorganisms in the flavonoids' biotransformation; for example, A. niger can transfer flavanone to flavan-4-ol, 2'-hydroxydihydrochalcone, flavone, 3-hydroxyflavone, 6-hydroxyflavanone, and 4'-hydroxyflavanone. The hydroxylation of flavones by microbes usually happens on the ortho position of hydroxyl group on the A ring and C-4' position of the B ring and microbes commonly hydroxylate flavonols at the C-8 position. The microorganisms tend to hydroxylate flavanones at the C-5, 6, and 4' positions; however, for prenylated flavanones, dihydroxylation often takes place on the C4α=C5α double bond on the prenyl group (the side chain of A ring). Isoflavones are usually hydroxylated at the C-3' position of the B ring by microorganisms. The microbes convert flavonoids to their 7-O-glycosides and 3-O-glycosides (when flavonoids have a hydroxyl moiety at the C-3 position). The demethylation of multimethoxyl flavonoids by microbes tends to happen at the C-3' and C-4' positions of the B ring. Multimethoxyl flavanones and isoflavone are demethylated at

  4. Enhanced bioactivity, biocompatibility and mechanical behavior of strontium substituted bioactive glasses.

    Science.gov (United States)

    Arepalli, Sampath Kumar; Tripathi, Himanshu; Hira, Sumit Kumar; Manna, Partha Pratim; Pyare, Ram; S P Singh

    2016-12-01

    Strontium contained biomaterials have been reported as a potential bioactive material for bone regeneration, as it reduces bone resorption and stimulates bone formation. In the present investigation, the bioactive glasses were designed to partially substitute SrO for SiO2 in Na2O-CaO-SrO-P2O5-SiO2 system. This work demonstrates that the substitution of SrO for SiO2 has got significant benefit than substitution for CaO in the bioactive glass. Bioactivity was assessed by the immersion of the samples in simulated body fluid for different intervals. The formation of hydroxy carbonate apatite layer was identified by X-ray diffractometry, scanning electron microscopy (SEM) and energy dispersive spectroscopy. The elastic modulus of the bioactive glasses was measured and found to increase with increasing SrO for SiO2. The blood compatibility of the samples was evaluated. In vitro cell culture studies of the samples were performed using human osteosarcoma U2-OS cell lines and found a significant improvement in cell viability and proliferation. The investigation showed enhancement in bioactivity, mechanical and biological properties of the strontia substituted for silica in glasses. Thus, these bioactive glasses would be highly potential for bone regeneration. Copyright © 2016 Elsevier B.V. All rights reserved.

  5. Enhanced bioactivity, biocompatibility and mechanical behavior of strontium substituted bioactive glasses

    Energy Technology Data Exchange (ETDEWEB)

    Arepalli, Sampath Kumar, E-mail: askumar.rs.cer11@iitbhu.ac.in [Department of Ceramic Engineering, Indian Institute of Technology (Banaras Hindu University), Varanasi 221005 (India); Tripathi, Himanshu [Department of Ceramic Engineering, Indian Institute of Technology (Banaras Hindu University), Varanasi 221005 (India); Hira, Sumit Kumar; Manna, Partha Pratim [Immunobiology Laboratory, Department of Zoology, Banaras Hindu University, Varanasi 221005 (India); Pyare, Ram; Singh, S.P. [Department of Ceramic Engineering, Indian Institute of Technology (Banaras Hindu University), Varanasi 221005 (India)

    2016-12-01

    Strontium contained biomaterials have been reported as a potential bioactive material for bone regeneration, as it reduces bone resorption and stimulates bone formation. In the present investigation, the bioactive glasses were designed to partially substitute SrO for SiO{sub 2} in Na{sub 2}O–CaO–SrO–P{sub 2}O{sub 5}–SiO{sub 2} system. This work demonstrates that the substitution of SrO for SiO{sub 2} has got significant benefit than substitution for CaO in the bioactive glass. Bioactivity was assessed by the immersion of the samples in simulated body fluid for different intervals. The formation of hydroxy carbonate apatite layer was identified by X-ray diffractometry, scanning electron microscopy (SEM) and energy dispersive spectroscopy. The elastic modulus of the bioactive glasses was measured and found to increase with increasing SrO for SiO{sub 2}. The blood compatibility of the samples was evaluated. In vitro cell culture studies of the samples were performed using human osteosarcoma U2-OS cell lines and found a significant improvement in cell viability and proliferation. The investigation showed enhancement in bioactivity, mechanical and biological properties of the strontia substituted for silica in glasses. Thus, these bioactive glasses would be highly potential for bone regeneration. - Highlights: • The substitution of SrO was done for SiO{sub 2} in Na{sub 2}O–CaO–SrO–P{sub 2}O{sub 5}–SiO{sub 2} bioactive glass. • Network connectivity significantly influenced on bioactivity and biocompatibility. • In vitro SBF studies showed enhanced HCA crystallinity on the glass surface. • The cell culture studies exhibited better cell compatibility and significant growth. • Density and elastic moduli increased with increasing concentration of strontia.

  6. Enhanced bioactivity, biocompatibility and mechanical behavior of strontium substituted bioactive glasses

    International Nuclear Information System (INIS)

    Arepalli, Sampath Kumar; Tripathi, Himanshu; Hira, Sumit Kumar; Manna, Partha Pratim; Pyare, Ram; Singh, S.P.

    2016-01-01

    Strontium contained biomaterials have been reported as a potential bioactive material for bone regeneration, as it reduces bone resorption and stimulates bone formation. In the present investigation, the bioactive glasses were designed to partially substitute SrO for SiO 2 in Na 2 O–CaO–SrO–P 2 O 5 –SiO 2 system. This work demonstrates that the substitution of SrO for SiO 2 has got significant benefit than substitution for CaO in the bioactive glass. Bioactivity was assessed by the immersion of the samples in simulated body fluid for different intervals. The formation of hydroxy carbonate apatite layer was identified by X-ray diffractometry, scanning electron microscopy (SEM) and energy dispersive spectroscopy. The elastic modulus of the bioactive glasses was measured and found to increase with increasing SrO for SiO 2 . The blood compatibility of the samples was evaluated. In vitro cell culture studies of the samples were performed using human osteosarcoma U2-OS cell lines and found a significant improvement in cell viability and proliferation. The investigation showed enhancement in bioactivity, mechanical and biological properties of the strontia substituted for silica in glasses. Thus, these bioactive glasses would be highly potential for bone regeneration. - Highlights: • The substitution of SrO was done for SiO 2 in Na 2 O–CaO–SrO–P 2 O 5 –SiO 2 bioactive glass. • Network connectivity significantly influenced on bioactivity and biocompatibility. • In vitro SBF studies showed enhanced HCA crystallinity on the glass surface. • The cell culture studies exhibited better cell compatibility and significant growth. • Density and elastic moduli increased with increasing concentration of strontia.

  7. Dietary Bioactive Diallyl Trisulfide in Cancer Prevention and Treatment.

    Science.gov (United States)

    Puccinelli, Michael T; Stan, Silvia D

    2017-07-28

    Bioactive dietary agents have been shown to regulate multiple cancer hallmark pathways. Epidemiologic studies have linked consumption of Allium vegetables, such as garlic and onions, to decreased incidence of cancer. Diallyl trisulfide (DATS), a bioactive compound derived from Allium vegetables, has been investigated as an anti-cancer and chemopreventive agent. Preclinical studies provide ample evidence that DATS regulates multiple cancer hallmark pathways including cell cycle, apoptosis, angiogenesis, invasion, and metastasis. DATS has been shown to arrest cancer cells at multiple stages of the cell cycle with the G2/M arrest being the most widely reported. Additionally, increased pro-apoptotic capacity as a result of regulating intrinsic and extrinsic apoptotic pathway components has been widely reported following DATS treatment. Invasion, migration, and angiogenesis represent emerging targets of DATS and support its anti-cancer properties. This review summarizes DATS mechanisms of action as an anti-cancer and chemopreventive agent. These studies provide rationale for future investigation into its use as a cancer chemopreventive agent.

  8. Correlations between chromatographic parameters and bioactivity predictors of potential herbicides.

    Science.gov (United States)

    Janicka, Małgorzata

    2014-08-01

    Different liquid chromatography techniques, including reversed-phase liquid chromatography on Purosphere RP-18e, IAM.PC.DD2 and Cosmosil Cholester columns and micellar liqud chromatography with a Purosphere RP-8e column and using buffered sodium dodecyl sulfate-acetonitrile as the mobile phase, were applied to study the lipophilic properties of 15 newly synthesized phenoxyacetic and carbamic acid derivatives, which are potential herbicides. Chromatographic lipophilicity descriptors were used to extrapolate log k parameters (log kw and log km) and log k values. Partitioning lipophilicity descriptors, i.e., log P coefficients in an n-octanol-water system, were computed from the molecular structures of the tested compounds. Bioactivity descriptors, including partition coefficients in a water-plant cuticle system and water-human serum albumin and coefficients for human skin partition and permeation were calculated in silico by ACD/ADME software using the linear solvation energy relationship of Abraham. Principal component analysis was applied to describe similarities between various chromatographic and partitioning lipophilicities. Highly significant, predictive linear relationships were found between chromatographic parameters and bioactivity descriptors. © The Author [2013]. Published by Oxford University Press. All rights reserved. For Permissions, please email: journals.permissions@oup.com.

  9. Micro-ion beam analysis of physico-chemical reactions in vitro induced by nano-structured sol-gel derived bioactive glasses; Caracterisation par micro-faisceau d'ions des reactions physico-chimiques induites in vitro par des verres bioactifs nanostructures elabores par la methode sol-gel

    Energy Technology Data Exchange (ETDEWEB)

    Lao, J

    2007-07-15

    The study of bioactive glasses is a multi-field area of research aiming at a major goal: the development of new generation biomaterials that would be able to bond with host tissues through the formation of a strong interfacial bond, together with helping the body heal itself through the stimulation of specific cellular responses. Thus clinical applications of bioactive glasses mainly concern dental surgery and orthopedics, for filling osseous defects. For this purpose, we have elaborated bioactive glasses in the binary SiO{sub 2}-CaO system, ternary SiO{sub 2}-CaO-P{sub 2}O{sub 5} system, and for the first time, to our knowledge, strontium-doped SiO{sub 2}-CaO-SrO and SiO{sub 2}-CaO-P{sub 2}O{sub 5}-SrO glasses. The materials were elaborated using the sol-gel process, which allowed the synthesis of nano-porous materials with great purity and homogeneity. The bio-activity of the glasses was clearly demonstrated in vitro: in contact with biological fluids, the whole lot of mate-rials were able to induce the formation of a Ca-P-Mg layer a few microns thick at their surface. Our work is characterized by the use of PIXE-RBS nuclear microprobes to study the bioactive glass/biological fluids interface. Thanks to these methods we obtained chemical maps that made possible the analysis of major and trace elements concentrations at the interface. Moreover, quantitative information regarding the local reactivity of glasses were acquired. These data are important to evaluate the kinetics and amplitude of the physico-chemical reactions involved in the bio-activity process. Thus, we highlighted that the binary glass is the highest reactive regarding the dissolution of the glassy matrix as well as the first appearance of the Ca-P rich layer. However the Ca/P atomic ratio calculated at the glass/biological fluids interface decreases slowly, indicating that the Ca-P-Mg layer encounters difficulties to be changed into a more stable apatitic phase. For the P-containing glasses, the de

  10. Surface coated polyurethane with improved bioactivity and cytocompatability

    CSIR Research Space (South Africa)

    Chetty, AS

    2006-02-01

    Full Text Available Polyurethane (PU) may be suitable for various implant applications; however, it lacks bioactivity. Bioactivity allows for direct tissue attachment at the bio- interface, enabling implant fixation while preventing fibrous encapsulation. To impart...

  11. Bioactive glass-based scaffolds for bone tissue engineering

    NARCIS (Netherlands)

    Will, J.; Gerhardt, L.C.; Boccaccini, A.R.

    2012-01-01

    Originally developed to fill and restore bone defects, bioactive glasses are currently also being intensively investigated for bone tissue engineering applications. In this chapter, we review and discuss current knowledge on porous bone tissue engineering scaffolds made from bioactive silicate

  12. Gastrointestinal Endogenous Proteins as a Source of Bioactive Peptides - An In Silico Study

    Science.gov (United States)

    Dave, Lakshmi A.; Montoya, Carlos A.; Rutherfurd, Shane M.; Moughan, Paul J.

    2014-01-01

    Dietary proteins are known to contain bioactive peptides that are released during digestion. Endogenous proteins secreted into the gastrointestinal tract represent a quantitatively greater supply of protein to the gut lumen than those of dietary origin. Many of these endogenous proteins are digested in the gastrointestinal tract but the possibility that these are also a source of bioactive peptides has not been considered. An in silico prediction method was used to test if bioactive peptides could be derived from the gastrointestinal digestion of gut endogenous proteins. Twenty six gut endogenous proteins and seven dietary proteins were evaluated. The peptides present after gastric and intestinal digestion were predicted based on the amino acid sequence of the proteins and the known specificities of the major gastrointestinal proteases. The predicted resultant peptides possessing amino acid sequences identical to those of known bioactive peptides were identified. After gastrointestinal digestion (based on the in silico simulation), the total number of bioactive peptides predicted to be released ranged from 1 (gliadin) to 55 (myosin) for the selected dietary proteins and from 1 (secretin) to 39 (mucin-5AC) for the selected gut endogenous proteins. Within the intact proteins and after simulated gastrointestinal digestion, angiotensin converting enzyme (ACE)-inhibitory peptide sequences were the most frequently observed in both the dietary and endogenous proteins. Among the dietary proteins, after in silico simulated gastrointestinal digestion, myosin was found to have the highest number of ACE-inhibitory peptide sequences (49 peptides), while for the gut endogenous proteins, mucin-5AC had the greatest number of ACE-inhibitory peptide sequences (38 peptides). Gut endogenous proteins may be an important source of bioactive peptides in the gut particularly since gut endogenous proteins represent a quantitatively large and consistent source of protein. PMID:24901416

  13. Gastrointestinal endogenous proteins as a source of bioactive peptides--an in silico study.

    Science.gov (United States)

    Dave, Lakshmi A; Montoya, Carlos A; Rutherfurd, Shane M; Moughan, Paul J

    2014-01-01

    Dietary proteins are known to contain bioactive peptides that are released during digestion. Endogenous proteins secreted into the gastrointestinal tract represent a quantitatively greater supply of protein to the gut lumen than those of dietary origin. Many of these endogenous proteins are digested in the gastrointestinal tract but the possibility that these are also a source of bioactive peptides has not been considered. An in silico prediction method was used to test if bioactive peptides could be derived from the gastrointestinal digestion of gut endogenous proteins. Twenty six gut endogenous proteins and seven dietary proteins were evaluated. The peptides present after gastric and intestinal digestion were predicted based on the amino acid sequence of the proteins and the known specificities of the major gastrointestinal proteases. The predicted resultant peptides possessing amino acid sequences identical to those of known bioactive peptides were identified. After gastrointestinal digestion (based on the in silico simulation), the total number of bioactive peptides predicted to be released ranged from 1 (gliadin) to 55 (myosin) for the selected dietary proteins and from 1 (secretin) to 39 (mucin-5AC) for the selected gut endogenous proteins. Within the intact proteins and after simulated gastrointestinal digestion, angiotensin converting enzyme (ACE)-inhibitory peptide sequences were the most frequently observed in both the dietary and endogenous proteins. Among the dietary proteins, after in silico simulated gastrointestinal digestion, myosin was found to have the highest number of ACE-inhibitory peptide sequences (49 peptides), while for the gut endogenous proteins, mucin-5AC had the greatest number of ACE-inhibitory peptide sequences (38 peptides). Gut endogenous proteins may be an important source of bioactive peptides in the gut particularly since gut endogenous proteins represent a quantitatively large and consistent source of protein.

  14. Chemotaxonomic Metabolite Profiling of 62 Indigenous Plant Species and Its Correlation with Bioactivities

    Directory of Open Access Journals (Sweden)

    Sarah Lee

    2015-11-01

    Full Text Available Chemotaxonomic metabolite profiling of 62 indigenous Korean plant species was performed by ultrahigh performance liquid chromatography (UHPLC-linear trap quadrupole-ion trap (LTQ-IT mass spectrometry/mass spectrometry (MS/MS combined with multivariate statistical analysis. In partial least squares discriminant analysis (PLS-DA, the 62 species clustered depending on their phylogenetic family, in particular, Aceraceae, Betulaceae, and Fagaceae were distinguished from Rosaceae, Fabaceae, and Asteraceae. Quinic acid, gallic acid, quercetin, quercetin derivatives, kaempferol, and kaempferol derivatives were identified as family-specific metabolites, and were found in relatively high concentrations in Aceraceae, Betulaceae, and Fagaceae. Fagaceae and Asteraceae were selected based on results of PLS-DA and bioactivities to determine the correlation between metabolic differences among plant families and bioactivities. Quinic acid, quercetin, kaempferol, quercetin derivatives, and kaempferol derivatives were found in higher concentrations in Fagaceae than in Asteraceae, and were positively correlated with antioxidant and tyrosinase inhibition activities. These results suggest that metabolite profiling was a useful tool for finding the different metabolic states of each plant family and understanding the correlation between metabolites and bioactivities in accordance with plant family.

  15. Accelerated bone ingrowth by local delivery of Zinc from bioactive ...

    African Journals Online (AJOL)

    2015-10-19

    Oct 19, 2015 ... Aims: This study aims to evaluate in vivo the performance therapy of zinc-doped bioactive glass (BG-Zn) and ... Keywords: zinc metallic ion; bioactive glass; osteoporosis; trabecular bone architecture; mechanical property; oxidative stress ..... Ducheyne P, Qiu Q. Bioactive ceramics: the effect of surface.

  16. Encapsulation for preservation of functionality and targeted delivery of bioactive food components

    NARCIS (Netherlands)

    de Vos, Paul; Faas, Marijke M.; Spasojevic, Milica; Sikkema, Jan

    There has been a tremendous increase in the number of food products containing bioactive components with a health promoting or disease preventing effect. Bioactive food components can be divided into bioactive molecules and bioactive living cells (probiotics). Both bioactive molecules and bioactive

  17. Vegetable foods: a cheap source of proteins and peptides with antihypertensive, antioxidant, and other less occurrence bioactivities.

    Science.gov (United States)

    García, M C; Puchalska, P; Esteve, C; Marina, M L

    2013-03-15

    Despite less explored than foods from animal origin, plant derived foods also contain biologically active proteins and peptides. Bioactive peptides can be present as an independent entity in the food or, more frequently, can be in a latent state as part of the sequence of a protein. Release from that protein requires protein hydrolysis by enzymatic digestion, fermentation or autolysis. Different methodologies have been used to test proteins and peptides bioactivities. Fractionation, separation, and identification techniques have also been employed for the isolation and identification of bioactive proteins or peptides. In this work, proteins and peptides from plant derived foods exerting antihypertensive, antioxidant, hypocholesterolemic, antithrombotic, and immunostimulating capacities or ability to reduce food intake have been reviewed. Copyright © 2013 Elsevier B.V. All rights reserved.

  18. Microstructures, hardness and bioactivity of hydroxyapatite coatings

    CSIR Research Space (South Africa)

    Tlotleng, Monnamme

    2014-10-01

    Full Text Available Hydroxyapatite (HAP) coatings on bioinert metals such as Ti–6Al–4V are necessary for biomedical applications. Together, HAP and Ti–6Al–4V are biocompatible and bioactive. The challenges of depositing HAP on Ti–6Al–4V with traditional thermal...

  19. Marine bioactives and potential application in sports.

    Science.gov (United States)

    Gammone, Maria Alessandra; Gemello, Eugenio; Riccioni, Graziano; D'Orazio, Nicolantonio

    2014-04-30

    An enriched diet with antioxidants, such as vitamin E, vitamin C, β-carotene and phenolic compounds, has always been suggested to improve oxidative stress, preventing related diseases. In this respect, marine natural product (MNP), such as COX inhibitors, marine steroids, molecules interfering with factors involved in the modulation of gene expression (such as NF-κB), macrolides, many antioxidant agents, thermogenic substances and even substances that could help the immune system and that result in the protection of cartilage, have been recently gaining attention. The marine world represents a reserve of bioactive ingredients, with considerable potential as functional food. Substances, such as chitin, chitosan, n-3 oils, carotenoids, vitamins, minerals and bioactive peptides, can provide several health benefits, such as the reduction of cardiovascular diseases, anti-inflammatory and anticarcinogenic activities. In addition, new marine bioactive substances with potential anti-inflammatory, antioxidant and thermogenic capacity may provide health benefits and performance improvement, especially in those who practice physical activity, because of their increased free radical and Reacting Oxygen Species (ROS) production during exercise, and, particularly, in athletes. The aim of this review is to examine the potential pharmacological properties and application of many marine bioactive substances in sports.

  20. Bioactive Compounds And Encapsulation Of Yanang ( Tiliacora ...

    African Journals Online (AJOL)

    Furthermore, this paper reports the design of the experimental method for optimization of Yanang encapsulation using three independent variables: the ratio of core material (Yanang), to wall material (gum Arabic), gum Arabic concentration and inlet temperature of spray drying on bioactive compounds stability. The stability ...

  1. Natural bioactive compounds: antibiotics | Dezfully | Journal of ...

    African Journals Online (AJOL)

    Antibiotics are powerful therapeutic agents that are produced by diverse living organisms. Over the last several decades, natural bioactive products particularly antibiotics have continued to play a significant role in drug discovery and has expanded the process for developing drugs with high degree of therapeutic index and ...

  2. Extraction, Isolation And Characterization Of Bioactive Compounds ...

    African Journals Online (AJOL)

    Natural products from medicinal plants, either as pure compounds or as standardized extracts, provide unlimited opportunities for new drug leads because of the ... The analysis of bioactive compounds present in the plant extracts involving the applications of common phytochemical screening assays, chromatographic ...

  3. Mechanical properties of bioactive glass putty formulations

    NARCIS (Netherlands)

    van Gestel, N.A.P.; Geurts, J.A.P.; Hulsen, D.J.W.; Hofmann, S.; Ito, K.; van Rietbergen, B.; Arts, J.J.C.

    2016-01-01

    Introduction: Bioactive glass (BAG) has been studied widely and seems to be a very promising biomaterial in regeneration of large bone defects and osteomyelitis treatment, because of its bone bonding and antibacterial properties[1]-[5]. Its high stiffness could potentially also enable mechanical

  4. Bioactive compounds in whole grain wheat

    NARCIS (Netherlands)

    Mateo Anson, N.

    2010-01-01

    Bread can be healthier! Consuming whole-grain foods can prevent cardiovascular diseases, type-2 diabetes and metabolic syndrome. This is due to bioactive compounds in whole grain, such as antioxidants and anti-inflammatory compounds. We found that the different fractions of a wheat grain vary much

  5. Legume bioactive compounds: influence of rhizobial inoculation

    Directory of Open Access Journals (Sweden)

    Luis R. Silva

    2017-04-01

    Full Text Available Legumes consumption has been recognized as beneficial for human health, due to their content in proteins, fiber, minerals and vitamins, and their cultivation as beneficial for sustainable agriculture due to their ability to fix atmospheric nitrogen in symbiosis with soil bacteria known as rhizobia. The inoculation with these baceria induces metabolic changes in the plant, from which the more studied to date are the increases in the nitrogen and protein contents, and has been exploited in agriculture to improve the crop yield of several legumes. Nevertheless, legumes also contain several bioactive compounds such as polysaccharides, bioactive peptides, isoflavones and other phenolic compounds, carotenoids, tocopherols and fatty acids, which makes them functional foods included into the nutraceutical products. Therefore, the study of the effect of the rhizobial inoculation in the legume bioactive compounds content is gaining interest in the last decade. Several works reported that the inoculation of different genera and species of rhizobia in several grain legumes, such as soybean, cowpea, chickpea, faba bean or peanut, produced increases in the antioxidant potential and in the content of some bioactive compounds, such as phenolics, flavonoids, organic acids, proteins and fatty acids. Therefore, the rhizobial inoculation is a good tool to enhance the yield and quality of legumes and further studies on this field will allow us to have plant probiotic bacteria that promote the plant growth of legumes improving their functionality.

  6. Preparation and bioactive properties of nano bioactive glass and segmented polyurethane composites.

    Science.gov (United States)

    Aguilar-Pérez, Fernando J; Vargas-Coronado, Rossana F; Cervantes-Uc, Jose M; Cauich-Rodríguez, Juan V; Covarrubias, Cristian; Pedram-Yazdani, Merhdad

    2016-04-01

    Composites of glutamine-based segmented polyurethanes with 5 to 25 wt.% bioactive glass nanoparticles were prepared, characterized, and their mineralization potential was evaluated in simulated body fluid. Biocompatibility with dental pulp stem cells was assessed by MTS to an extended range of compositions (1 to 25 wt.% of bioactive glass nanoparticles). Physicochemical characterization showed that composites retained many of the matrix properties, i.e. those corresponding to semicrystalline elastomeric polymers as they exhibited a glass transition temperature (Tg) between -41 and -36℃ and a melting temperature (Tm) between 46 and 49℃ in agreement with X-ray reflections at 23.6° and 21.3°. However, with bioactive glass nanoparticles addition, tensile strength and strain were reduced from 22.2 to 12.2 MPa and 667.2 to 457.8%, respectively with 25 wt.% of bioactive glass nanoparticles. Although Fourier transform infrared spectroscopy did not show evidence of mineralization after conditioning of these composites in simulated body fluid, X-ray diffraction, scanning electron microscopy, and energy dispersive X-ray microanalysis showed the formation of an apatite layer on the surface which increased with higher bioactive glass concentrations and longer conditioning time. Dental pulp stem cells proliferation at day 5 was improved in bioactive glass nanoparticles composites containing lower amounts of the filler (1-2.5 wt.%) but it was compromised at day 9 in composites containing high contents of nBG (5, 15, 25 wt.%). However, Runx2 gene expression was particularly upregulated for the dental pulp stem cells cultured with composites loaded with 15 and 25 wt.% of bioactive glass nanoparticles. In conclusion, low content bioactive glass nanoparticles and segmented polyurethanes composites deserve further investigation for applications such as guided bone regeneration membranes, where osteoconductivity is desirable but not a demanding mechanical performance. © The

  7. Plasma spraying of bioactive glass-ceramics containing bovine bone

    Directory of Open Access Journals (Sweden)

    Annamária Dobrádi

    2017-06-01

    Full Text Available Natural bone derived glass-ceramics are promising biomaterials for implants. However, due to their price and weak mechanical properties they are preferably applied as coatings on load bearing implants. This paper describes result obtained by plasma spraying of bioactive glass-ceramics containing natural bone onto selected implant materials, such as stainless steel, alumina, and titanium alloy. Adhesion of plasma sprayed coating was tested by computed X-ray tomography and SEM of cross sections. The results showed defect free interface between the coating and substrate, without cracks or gaps. Dissolution rate of the coating in simulated body fluid (SBF was readily controlled by the bone additives (phase composition, as well as microstructure. The SBF treatment of the plasma sprayed coating did not influence the boundary between the coating and substrate.

  8. Thermal analysis and in vitro bioactivity of bioactive glass-alumina composites

    Energy Technology Data Exchange (ETDEWEB)

    Chatzistavrou, Xanthippi, E-mail: x.chatzistavrou@imperial.ac.uk [Solid State Physics Section, Physics Department, Aristotle University of Thessaloniki, 54124 Thessaloniki (Greece); Kantiranis, Nikolaos, E-mail: kantira@geo.auth.gr [School of Geology, Aristotle University of Thessaloniki, 54124 Thessaloniki (Greece); Kontonasaki, Eleana, E-mail: kont@dent.auth.gr [School of Dentistry, Department of Fixed Prosthesis and Implant Prosthodontics, Aristotle University of Thessaloniki, 54124 Thessaloniki (Greece); Chrissafis, Konstantinos, E-mail: hrisafis@physics.auth.gr [Solid State Physics Section, Physics Department, Aristotle University of Thessaloniki, 54124 Thessaloniki (Greece); Papadopoulou, Labrini, E-mail: lambrini@geo.auth.gr [School of Geology, Aristotle University of Thessaloniki, 54124 Thessaloniki (Greece); Koidis, Petros, E-mail: pkoidis@dent.auth.gr [School of Dentistry, Department of Fixed Prosthesis and Implant Prosthodontics, Aristotle University of Thessaloniki, 54124 Thessaloniki (Greece); Boccaccini, Aldo R., E-mail: a.boccaccini@imperial.ac.uk [Department of Materials, Faculty of Engineering, Imperial College, SW7 2AZ London (United Kingdom); Paraskevopoulos, Konstantinos M., E-mail: kpar@auth.gr [Solid State Physics Section, Physics Department, Aristotle University of Thessaloniki, 54124 Thessaloniki (Greece)

    2011-01-15

    Bioactive glass-alumina composite (BA) pellets were fabricated in the range 95/5-60/40 wt.% respectively and were heat-treated under a specific thermal treatment up to 950 {sup o}C. Control (unheated) and heat-treated pellets were immersed in Simulated Body Fluid (SBF) for bioactivity testing. All pellets before and after immersion in SBF were studied by Fourier Transform Infrared spectroscopy (FTIR), Scanning Electron Microscopy (SEM-EDS) and X-ray Diffraction (XRD) analysis. All composite pellets presented bioactive response. On the surface of the heat-treated pellets the development of a rich biological hydroxyapatite (HAp) layer was delayed for one day, compared to the respective control pellets. Independent of the proportion of the two components, all composites of each group (control and heat-treated) presented the same bioactive response as a function of immersion time in SBF. It was found that by the applied methodology, Al{sub 2}O{sub 3} can be successfully applied in bioactive glass composites without obstructing their bioactive response. - Research Highlights: {yields} Isostatically pressed glass-alumina composites presented apatite-forming ability. {yields} The interaction with SBF resulted in an aluminium phosphate phase formation. {yields} The formation of an aluminium phosphate phase enhanced the in vitro apatite growth.

  9. Experimental and Clinical Pharmacology of Andrographis paniculata and Its Major Bioactive Phytoconstituent Andrographolide

    Directory of Open Access Journals (Sweden)

    Thanasekaran Jayakumar

    2013-01-01

    Full Text Available Andrographis paniculata (Burm. F Nees, generally known as “king of bitters,” is an herbaceous plant in the family Acanthaceae. In China, India, Thailand, and Malaysia, this plant has been widely used for treating sore throat, flu, and upper respiratory tract infections. Andrographolide, a major bioactive chemical constituent of the plant, has shown anticancer potential in various investigations. Andrographolide and its derivatives have anti-inflammatory effects in experimental models asthma, stroke, and arthritis. In recent years, pharmaceutical chemists have synthesized numerous andrographolide derivatives, which exhibit essential pharmacological activities such as those that are anti-inflammatory, antibacterial, antitumor, antidiabetic, anti-HIV, antifeedant, and antiviral. However, what is noteworthy about this paper is summarizing the effects of andrographolide against cardiovascular disease, platelet activation, infertility, and NF-κB activation. Therefore, this paper is intended to provide evidence reported in relevant literature on qualitative research to assist scientists in isolating and characterizing bioactive compounds.

  10. Plant Bioactive Metabolites and Drugs Produced by Endophytic Fungi of Spermatophyta

    Directory of Open Access Journals (Sweden)

    Rosario Nicoletti

    2015-09-01

    Full Text Available It is known that plant-based ethnomedicine represented the foundation of modern pharmacology and that many pharmaceuticals are derived from compounds occurring in plant extracts. This track still stimulates a worldwide investigational activity aimed at identifying novel bioactive products of plant origin. However, the discovery that endophytic fungi are able to produce many plant-derived drugs has disclosed new horizons for their availability and production on a large scale by the pharmaceutical industry. In fact, following the path traced by the blockbuster drug taxol, an increasing number of valuable compounds originally characterized as secondary metabolites of plant species belonging to the Spermatophyta have been reported as fermentation products of endophytic fungal strains. Aspects concerning sources and bioactive properties of these compounds are reviewed in this paper.

  11. Experimental and Clinical Pharmacology of Andrographis paniculata and Its Major Bioactive Phytoconstituent Andrographolide

    Science.gov (United States)

    Jayakumar, Thanasekaran; Hsieh, Cheng-Ying; Lee, Jie-Jen; Sheu, Joen-Rong

    2013-01-01

    Andrographis paniculata (Burm. F) Nees, generally known as “king of bitters,” is an herbaceous plant in the family Acanthaceae. In China, India, Thailand, and Malaysia, this plant has been widely used for treating sore throat, flu, and upper respiratory tract infections. Andrographolide, a major bioactive chemical constituent of the plant, has shown anticancer potential in various investigations. Andrographolide and its derivatives have anti-inflammatory effects in experimental models asthma, stroke, and arthritis. In recent years, pharmaceutical chemists have synthesized numerous andrographolide derivatives, which exhibit essential pharmacological activities such as those that are anti-inflammatory, antibacterial, antitumor, antidiabetic, anti-HIV, antifeedant, and antiviral. However, what is noteworthy about this paper is summarizing the effects of andrographolide against cardiovascular disease, platelet activation, infertility, and NF-κB activation. Therefore, this paper is intended to provide evidence reported in relevant literature on qualitative research to assist scientists in isolating and characterizing bioactive compounds. PMID:23634174

  12. Antibacterial effect of bioactive glasses on clinically important anaerobic bacteria in vitro.

    Science.gov (United States)

    Leppäranta, Outi; Vaahtio, Minna; Peltola, Timo; Zhang, Di; Hupa, Leena; Hupa, Mikko; Ylänen, Heimo; Salonen, Jukka I; Viljanen, Matti K; Eerola, Erkki

    2008-02-01

    Bioactive glasses (BAGs) of different compositions have been studied for decades for clinical use and they have found many dental and orthopaedic applications. Particulate BAGs have also been shown to have antibacterial properties. This large-scale study shows that two bioactive glass powders (S53P4 and 13-93) and a sol-gel derived material (CaPSiO II) have an antibacterial effect on 17 clinically important anaerobic bacterial species. All the materials tested demonstrated growth inhibition, although the concentration and time needed for the effect varied depending on the BAG. Glass S53P4 had a strong growth-inhibitory effect on all pathogens tested. Glass 13-93 and sol-gel derived material CaPSiO II showed moderate antibacterial properties.

  13. Retinal expression, regulation, and functional bioactivity of prostacyclin-stimulating factor

    OpenAIRE

    Hata, Yasuaki; Clermont, Allen Charles; Yamauchi, Teruaki; Pierce, Eric Adam; Suzuma, Izumi; Kagokawa, Hiroyuki; Yoshikawa, Hiroshi; Robinson, Gregory S.; Ishibashi, Tatsuro; Hashimoto, Toshihiko; Umeda, Fumio; Bursell, Sven E.; Aiello, Lloyd Paul

    2000-01-01

    Prostacyclin-stimulating factor (PSF) acts on vascular endothelial cells to stimulate the synthesis of the vasodilatory molecule prostacyclin (PGI2). We have examined the expression, regulation, and hemodynamic bioactivity of PSF both in whole retina and in cultured cells derived from this tissue. PSF was expressed in all retinal cell types examined in vitro, but immunohistochemical analysis revealed PSF mainly associated with retinal vessels. PSF expression was constitutive in retinal pericy...

  14. Bioactivity characterization of 45S5 bioglass using TL, OSL and EPR: Comparison with the case of 58S sol-gel bioactive glass

    Energy Technology Data Exchange (ETDEWEB)

    Polymeris, G.S., E-mail: gspolymeris@ankara.edu.tr [Ankara University, Institute of Nuclear Sciences, 06100 Beşevler, Ankara (Turkey); Giannoulatou, V. [Ankara University, Institute of Nuclear Sciences, 06100 Beşevler, Ankara (Turkey); Solid State Section, Department of Physics, Aristotle University of Thessaloniki, 54124 Thessaloniki (Greece); Kyriakidou, A. [Solid State Section, Department of Physics, Aristotle University of Thessaloniki, 54124 Thessaloniki (Greece); Sfampa, I.K. [Nuclear Physics Laboratory, Department of Physics, Aristotle University of Thessaloniki, 54124 Thessaloniki (Greece); Theodorou, G.S. [Solid State Section, Department of Physics, Aristotle University of Thessaloniki, 54124 Thessaloniki (Greece); Şahiner, E.; Meriç, N. [Ankara University, Institute of Nuclear Sciences, 06100 Beşevler, Ankara (Turkey); Kitis, G. [Nuclear Physics Laboratory, Department of Physics, Aristotle University of Thessaloniki, 54124 Thessaloniki (Greece); Paraskevopoulos, K.M. [Solid State Section, Department of Physics, Aristotle University of Thessaloniki, 54124 Thessaloniki (Greece)

    2017-01-01

    of the 58S sol-gel bioactive glass, in terms of the timescale of these five stages required for the final formation of the HCAp. The techniques of luminescence and EPR which take advantage of trapped charges are proposed as alternative cheap and prompt effective techniques towards discrimination between different bioactive responses in bioactive glasses. - Highlights: • TL, OSL and EPR have been applied as alternative techniques for bioactivity characteriztion. • The 110 °C TL peak and the peak to peak intensity of the OHC EPR signal have been effectively considered as proxies for bioactivity studies. • A time scale has been established for each chemical reaction involved in the five-step procedure required for the HCAp formation. • Besides the first initial step, the beginning of the rest chemical reaction steps takes place faster in the case of sol-gel derived 58S glass than the quenching-derived 45S5 bioglass.

  15. Photoreactive elastin-like proteins for use as versatile bioactive materials and surface coatings.

    Science.gov (United States)

    Raphel, Jordan; Parisi-Amon, Andreina; Heilshorn, Sarah

    2012-10-07

    Photocrosslinkable, protein-engineered biomaterials combine a rapid, controllable, cytocompatible crosslinking method with a modular design strategy to create a new family of bioactive materials. These materials have a wide range of biomedical applications, including the development of bioactive implant coatings, drug delivery vehicles, and tissue engineering scaffolds. We present the successful functionalization of a bioactive elastin-like protein with photoreactive diazirine moieties. Scalable synthesis is achieved using a standard recombinant protein expression host followed by site-specific modification of lysine residues with a heterobifunctional N-hydroxysuccinimide ester-diazirine crosslinker. The resulting biomaterial is demonstrated to be processable by spin coating, drop casting, soft lithographic patterning, and mold casting to fabricate a variety of two- and three-dimensional photocrosslinked biomaterials with length scales spanning the nanometer to millimeter range. Protein thin films proved to be highly stable over a three-week period. Cell-adhesive functional domains incorporated into the engineered protein materials were shown to remain active post-photo-processing. Human adipose-derived stem cells achieved faster rates of cell adhesion and larger spread areas on thin films of the engineered protein compared to control substrates. The ease and scalability of material production, processing versatility, and modular bioactive functionality make this recombinantly engineered protein an ideal candidate for the development of novel biomaterial coatings, films, and scaffolds.

  16. Effect of enzymatic hydrolysis on bioactive properties and allergenicity of cricket (Gryllodes sigillatus) protein.

    Science.gov (United States)

    Hall, Felicia; Johnson, Philip E; Liceaga, Andrea

    2018-10-01

    Food-derived bioactive peptides have gained attention for their role in preventing chronic diseases. Edible insects are viable sources of bioactive peptides owing to their high protein content and sustainable production. In this study, whole crickets (Gryllodes sigillatus) were alcalase-hydrolyzed to a degree of hydrolysis (DH) ranging from 15 to 85%. Antioxidant activity, angiotensin converting enzyme (ACE), and dipeptidyl peptidase-4 (DPP-IV)- inhibition of the cricket protein hydrolysates (CPH) were evaluated before and after simulated gastrointestinal digestion (SGD). Antioxidant activity was similar among CPH, whereas ACE and DPP-IV inhibition was greater (p < 0.05) in CPH with 60-85% DH. Bioactivity improved after SGD. CPH allergenicity was evaluated using human shrimp-allergic sera. All sera positively reacted to tropomyosin in the unhydrolyzed cricket and CPH with 15-50% DH, whereas 60-85% DH showed no reactivity. In conclusion, CPH (60-85% DH) had the greatest bioactive potential and lowest reactivity to tropomyosin, compared with other CPH and the unhydrolyzed control. Copyright © 2018 Elsevier Ltd. All rights reserved.

  17. Composition of amino acids and bioactive amines in common wines of Brazil

    Directory of Open Access Journals (Sweden)

    Bruna Carla Agustini

    2014-10-01

    Full Text Available Since most consumed wines in Brazil are common wines and since their representativeness is not accounted for in scientific research, current study quantifies bioactive amines and their precursors in Brazilian sweet and dry common wines, correlates the formation of amines with physical and chemical parameters and clusters studied areas by their amine and amino acid contents. Forty-seven wine samples varying in type, color and origin were analyzed simultaneously for seventeen amino acids, ammonium ion and five bioactive amines by reversed-phase high performance liquid chromatography and ultraviolet detection after the derivation phase. Physical and chemical analyses comprised titratable acidity, pH, organic acids, sugar and alcohol contents. Sweet wines had lower concentrations of amino acids and bioactive amines. Dry white wines had higher amino acid contents when compared to those in dry red wines. Since multivariate data analysis confirmed similarities between the studied regions, their unity as potential viniculture area was reinforced. Amine levels in Brazilian common wines were reported for the first time and results reinforced the importance of bioactive amines quantification and the use of suitable vinification practices to reduce their formation.

  18. MECANISMUL DE PROTEOLIZĂ A FICOCIANINEI, PROTEINEI BIOACTIVE DIN SPIRULINĂ SUB ACŢIUNEA PAPAINEI

    Directory of Open Access Journals (Sweden)

    Angela RUDAKOVA

    2016-02-01

    Full Text Available Elaborarea unor procedee de obţinere a peptidelor bioactive din ficocianină prin intermediul hidrolizei proteolitice prezintă un interes sporit pentru cercetători în contextul utilizării acestora în calitate de remedii anticancer şi pentru alte proprietăţi terapeutice. Peptidele derivate din ficocianină ar putea manifesta proprietăţi terapeutice mult mai pronunţate comparativ cu ficocianina. În prezenta lucrare sunt studiate dinamica proteolizei ficocianinei cu papaina şi mecanismul de hidroliză a acestei proteine.Mechanism of proteolysis of C-phycocyanin, bioactive protein from Spirulina, under the action of papainThe elaboration of the procedures of obtaining of bioactive peptides derived from phycocyanin, as a result of it proteolytic hydrolysis presents great interest for researchers in the terms of theirs use as anti-cancer drugs and for other therapeutic properties. It can be assumed that peptides derived from phycocyanin could manifest more pronounced therapeutic effects compared to phycocyanin. Dynamics of phycocyanin proteolisis by papain, as well as mechanism of phycocyanin hydrolysis were studied in the present work. 

  19. Influence of barium substitution on bioactivity, thermal and physico-mechanical properties of bioactive glass

    Energy Technology Data Exchange (ETDEWEB)

    Arepalli, Sampath Kumar, E-mail: askumar.rs.cer11@iitbhu.ac.in; Tripathi, Himanshu; Vyas, Vikash Kumar; Jain, Shubham; Suman, Shyam Kumar; Pyare, Ram; Singh, S.P., E-mail: spsinghceram@gmail.com

    2015-04-01

    Barium with low concentration in the glasses acts as a muscle stimulant and is found in human teeth. We have made a primary study by substituting barium in the bioactive glass. The chemical composition containing (46.1 − X) SiO{sub 2−}–24.3 Na{sub 2}O–26.9 CaO–2.6 P{sub 2}O{sub 5}, where X = 0, 0.4, 0.8, 1.2 and 1.6 mol% of BaO was chosen and melted in an electric furnace at 1400 ± 5 °C. The glasses were characterized to determine their use in biomedical applications. The nucleation and crystallization regimes were determined by DTA and the controlled crystallization was carried out by suitable heat treatment. The crystalline phase formed was identified by using XRD technique. Bioactivity of these glasses was assessed by immersion in simulated body fluid (SBF) for various time periods. The formation of hydroxy carbonate apatite (HCA) layer was identified by FTIR spectrometry, scanning electron microscope (SEM) and XRD which showed the presence of HCA as the main phase in all tested bioactive glass samples. Flexural strength and densities of bioactive glasses have been measured and found to increase with increasing the barium content. The human blood compatibility of the samples was evaluated and found to be pertinent. - Highlights: • In vitro bioactivity of soda-lime–baria-phospho-silicate glass was investigated. • HCA formed on surface of glasses was confirmed by XRD, SEM and FTIR spectrometry. • Mechanical properties of glasses were found to increase with barium addition. • Hemolysis showed that 1.2 mol% BaO bioactive glass exhibited better biocompatibility. • Barium substituted bioactive glasses can be used as bone implants.

  20. Novel injectable gellan gum hydrogel composites incorporating Zn- and Sr-enriched bioactive glass microparticles: High-resolution X-ray microcomputed tomography, antibacterial and in vitro testing.

    Science.gov (United States)

    Douglas, Timothy E L; Dziadek, Michal; Gorodzha, Svetlana; Lišková, Jana; Brackman, Gilles; Vanhoorne, Valérie; Vervaet, Chris; Balcaen, Lieve; Del Rosario Florez Garcia, Maria; Boccaccini, Aldo R; Weinhardt, Venera; Baumbach, Tilo; Vanhaecke, Frank; Coenye, Tom; Bačáková, Lucie; Surmeneva, Maria A; Surmenev, Roman A; Cholewa-Kowalska, Katarzyna; Skirtach, Andre G

    2018-06-01

    Mineralization of hydrogel biomaterials is desirable to improve their suitability as materials for bone regeneration. In this study, gellan gum (GG) hydrogels were formed by simple mixing of GG solution with bioactive glass microparticles of 45S5 composition, leading to hydrogel formation by ion release from the amorphous bioactive glass microparticles. This resulted in novel injectable, self-gelling composites of GG hydrogels containing 20% bioactive glass. Gelation occurred within 20 min. Composites containing the standard 45S5 bioactive glass preparation were markedly less stiff. X-ray microcomputed tomography proved to be a highly sensitive technique capable of detecting microparticles of diameter approximately 8 μm, that is, individual microparticles, and accurately visualizing the size distribution of bioactive glass microparticles and their aggregates, and their distribution in GG hydrogels. The widely used melt-derived 45S5 preparation served as a standard and was compared with a calcium-rich, sol-gel derived preparation (A2), as well as A2 enriched with zinc (A2Zn5) and strontium (A2Sr5). A2, A2Zn, and A2Sr bioactive glass particles were more homogeneously dispersed in GG hydrogels than 45S5. Composites containing all four bioactive glass preparations exhibited antibacterial activity against methicillin-resistant Staphylococcus aureus. Composites containing A2Zn5 and A2Sr5 bioactive glasses supported the adhesion and growth of osteoblast-like cells and were considerably more cytocompatible than 45S5. All composites underwent mineralization with calcium-deficient hydroxyapatite upon incubation in simulated body fluid. The extent of mineralization appeared to be greatest for composites containing A2Zn5 and 45S5. The results underline the importance of the choice of bioactive glass when preparing injectable, self-gelling composites. Copyright © 2018 John Wiley & Sons, Ltd.

  1. Peptidome characterization and bioactivity analysis of donkey milk.

    Science.gov (United States)

    Piovesana, Susy; Capriotti, Anna Laura; Cavaliere, Chiara; La Barbera, Giorgia; Samperi, Roberto; Zenezini Chiozzi, Riccardo; Laganà, Aldo

    2015-04-24

    Donkey milk is an interesting commercial product for its nutritional values, which make it the most suitable mammalian milk for human consumption, and for the bioactivity associated with it and derivative products. To further mine the characterization of donkey milk, an extensive peptidomic study was performed. Two peptide purification strategies were compared to remove native proteins and lipids and enrich the peptide fraction. In one case the whole protein content was precipitated by organic solvent using cold acetone. In the other one the precipitation of the most abundant milk proteins, caseins, was performed under acidic conditions by acetic acid at pH4.6, instead. The procedures were compared and proved to be partially complementary. Considered together they provided 1330 peptide identifications for donkey milk, mainly coming from the most abundant proteins in milk. The bioactivity of the isolated peptides was also investigated, both by angiotensin-converting-enzyme inhibitory and antioxidant activity assays and by bioinformatics, proving that the isolated peptides did have the tested biological activities. The rationale behind this study is that peptides in food matrices often play an important biological role and, despite the extensive study of the protein composition of different samples, they remain poorly characterized. In fact, in a typical shotgun proteomics study endogenous peptides are not properly characterized. In proteomics workflows one limiting point is the isolation process: if it is specific for the purification of proteins, it often comprises a precipitation step which aims at isolating pure protein pellets and remove unwonted interferent compounds. In this way endogenous peptides, which are not effectively precipitated as well as proteins, are removed too and not analyzed at the end of the process. Moreover, endogenous peptides do often originate from precursor proteins, but in phenomena which are independent of the shotgun digestion

  2. Bioactive Compounds in Functional Meat Products.

    Science.gov (United States)

    Pogorzelska-Nowicka, Ewelina; Atanasov, Atanas G; Horbańczuk, Jarosław; Wierzbicka, Agnieszka

    2018-01-31

    Meat and meat products are a good source of bioactive compounds with positive effect on human health such as vitamins, minerals, peptides or fatty acids. Growing food consumer awareness and intensified global meat producers competition puts pressure on creating new healthier meat products. In order to meet these expectations, producers use supplements with functional properties for animal diet and as direct additives for meat products. In the presented work seven groups of key functional constituents were chosen: (i) fatty acids; (ii) minerals; (iii) vitamins; (iv) plant antioxidants; (v) dietary fibers; (vi) probiotics and (vii) bioactive peptides. Each of them is discussed in term of their impact on human health as well as some quality attributes of the final products.

  3. Microgreens: Production, shelf life, and bioactive components.

    Science.gov (United States)

    Mir, Shabir Ahmad; Shah, Manzoor Ahmad; Mir, Mohammad Maqbool

    2017-08-13

    Microgreens are emerging specialty food products which are gaining popularity and increased attention nowadays. They are young and tender cotyledonary leafy greens that are found in a pleasing palette of colors, textures, and flavors. Microgreens are a new class of edible vegetables harvested when first leaves have fully expanded and before true leaves have emerged. They are gaining popularity as a new culinary ingredient. They are used to enhance salads or as edible garnishes to embellish a wide variety of other dishes. Common microgreens are grown mainly from mustard, cabbage, radish, buckwheat, lettuce, spinach, etc. The consumption of microgreens has nowadays increased due to higher concentrations of bioactive components such as vitamins, minerals, and antioxidants than mature greens, which are important for human health. However, they typically have a short shelf life due to rapid product deterioration. This review aimed to evaluate the postharvest quality, potential bioactive compounds, and shelf life of microgreens for proper management of this specialty produce.

  4. Bioactive Compounds in Functional Meat Products

    OpenAIRE

    Ewelina Pogorzelska-Nowicka; Atanas G. Atanasov; Jarosław Horbańczuk; Agnieszka Wierzbicka

    2018-01-01

    Meat and meat products are a good source of bioactive compounds with positive effect on human health such as vitamins, minerals, peptides or fatty acids. Growing food consumer awareness and intensified global meat producers competition puts pressure on creating new healthier meat products. In order to meet these expectations, producers use supplements with functional properties for animal diet and as direct additives for meat products. In the presented work seven groups of key functional cons...

  5. Secondary metabolites and bioactivities of Myrtus communis

    OpenAIRE

    Mahmoud I Nassar; El-Sayed A Aboutabl; Rania F Ahmed; Ezzel-Din A El-Khrisy; Khaled M Ibrahim; Amany A Sleem

    2010-01-01

    Background: Myrtus species are characterized by the presence of phenolic acids, flavonoids, tannins, volatile oils and fatty acids. They are remedies for variety of ailments. This study therefore investigated medicinal effects of Myrtus communis L. Methods: Bioactivity studies of Myrtus communis L. leaves were carried out on volatile oil, 7% methanol and aqueous extracts and the isolated compounds myricetin 3-O-β-glucopyranoside, myricetin 3-O-∝-rhamnopyranoside and gallic acid. Results: Dete...

  6. Development of bioactive materials for glioblastoma therapy

    Directory of Open Access Journals (Sweden)

    Jun Yang

    2016-09-01

    Full Text Available Glioblastoma is the most common and deadly human brain cancers. Unique barriers hinder the drug delivering pathway due to the individual position of glioblastoma, including blood-brain barrier and blood-brain tumor barrier. Numerous bioactive materials have been exploited and applied as the transvascular delivery carriers of therapeutic drugs. They promote site-specific accumulation and long term release of the encapsulated drugs at the tumor sites and reduce side effects with systemic delivery. And the delivery systems exhibit a certain extent of anti-glioblastoma effect and extend the median survival time. However, few of them step into the clinical trials. In this review, we will investigate the recent studies of bioactive materials for glioblastoma chemotherapy, including the inorganic materials, lipids and polymers. These bioactive materials construct diverse delivery vehicles to trigger tumor sites in brain intravenously. Herein, we exploit their functionality in drug delivery and discuss the deficiency for the featured tumors, to provide guidance for establishing optimized therapeutic drug formulation for anti-glioblastoma therapy and pave the way for clinical application.

  7. A new bio-active glass ceramic

    International Nuclear Information System (INIS)

    Shamim, A.; Arif, I.; Suleman, M.; Hussain, K.; Shah, W.A.

    1995-01-01

    Since 1960 fine ceramics such as alumina have been used side by side with metallic materials for bone and joint replacement. They have high mechanical strength and are free from corrosion problem faced by metals. However they don't bond to the natural living bone and hence are called bio-inactive. This was followed by the development of bio-active glasses and glass-ceramics which bond to the natural bone but have low mechanical strength. In the present work a new bio-active glass-ceramic, based on CaO-SiO/sub 2/-P/sub 2/O/sub 3/-MgO composition, has been developed which has mechanical strength compared to that of a bio-inactive glass ceramic and also bonds strongly to the natural bone. X-ray diffraction analysis reveals wollastanite and apatite phases in the glass ceramic. A new bio-active cement has also been developed which can be used to join broken pieces of bone or by itself at a filler. (author)

  8. Adhesive Bioactive Coatings Inspired by Sea Life.

    Science.gov (United States)

    Rego, Sónia J; Vale, Ana C; Luz, Gisela M; Mano, João F; Alves, Natália M

    2016-01-19

    Inspired by nature, in particular by the marine mussels adhesive proteins (MAPs) and by the tough brick-and-mortar nacre-like structure, novel multilayered films are prepared in the present work. Organic-inorganic multilayered films, with an architecture similar to nacre based on bioactive glass nanoparticles (BG), chitosan, and hyaluronic acid modified with catechol groups, which are the main components responsible for the outstanding adhesion in MAPs, are developed for the first time. The biomimetic conjugate is prepared by carbodiimide chemistry and analyzed by ultraviolet-visible spectrophotometry. The buildup of the multilayered films is monitored with a quartz crystal microbalance with dissipation monitoring, and their topography is characterized by atomic force microscopy. The mechanical properties reveal that the films containing catechol groups and BG present an enhanced adhesion. Moreover, the bioactivity of the films upon immersion in a simulated body fluid solution is evaluated by scanning electron microscopy coupled with energy dispersive X-ray spectroscopy, Fourier transform infrared spectroscopy, and X-ray diffraction. It was found that the constructed films promote the formation of bonelike apatite in vitro. Such multifunctional mussel inspired LbL films, which combine enhanced adhesion and bioactivity, could be potentially used as coatings of a variety of implants for orthopedic applications.

  9. Human Milk Composition: Nutrients and Bioactive Factors

    Science.gov (United States)

    Ballard, Olivia; Morrow, Ardythe L.

    2013-01-01

    Synopsis The composition of human milk is the biologic norm for infant nutrition. Human milk also contains many hundreds to thousands of distinct bioactive molecules that protect against infection and inflammation and contribute to immune maturation, organ development, and healthy microbial colonization. Some of these molecules, e.g., lactoferrin, are being investigated as novel therapeutic agents. A dynamic, bioactive fluid, human milk changes in composition from colostrum to late lactation, and varies within feeds, diurnally, and between mothers. Feeding infants with expressed human milk is increasing. Pasteurized donor milk is now commonly provided to high risk infants and most mothers in the U.S. express and freeze their milk at some point in lactation for future infant feedings. Many milk proteins are degraded by heat treatment and freeze-thaw cycles may not have the same bioactivity after undergoing these treatments. This article provides an overview of the composition of human milk, sources of its variation, and its clinical relevance. PMID:23178060

  10. Ultrasound assisted extraction of bioactive compounds

    Directory of Open Access Journals (Sweden)

    Helena Drmić

    2010-01-01

    Full Text Available Many novel and innovative techniques are nowadays researched and explored in order to replace or improve classical, thermal processing technologies. One of newer technique is technique of minimal food processing, under what we assume ultrasound processing. Ultrasound technology can be very useful for minimal food processing because transmission of acoustic energy through product is fast and complete, which allows reduction in total processing time, and therefore lower energy consumption. Industrial processing is growing more and more waste products, and in desire of preservation of global recourses and energy efficiency, several ways of active compounds extraction techniques are now explored. The goal is to implement novel extraction techniques in food and pharmaceutical industry as well in medicine. Ultrasound assisted extraction of bioactive compounds offers increase in yield, and reduction or total avoiding of solvent usage. Increase in temperature of treatment is controlled and restricted, thereby preserving extracted bioactive compounds. In this paper, several methods of ultrasound assisted extraction of bioactive compounds from plant materials are shown. Ultrasound can improve classic mechanisms of extraction, and thereby offer novel possibilities of commercial extraction of desired compounds. Application of sonochemistry (ultrasound chemistry is providing better yield in desired compounds and reduction in treatment time.

  11. EFFECTS OF INCORPORATING NATURAL MINERALS ON PRODUCTION AND BIOACTIVITY OF BIOACTIVE GLASS CERAMICS

    Directory of Open Access Journals (Sweden)

    Franco Matias Stabile

    2016-07-01

    Full Text Available Two glass-ceramics composition were produced from natural minerals. Quartzes and feldspars were pre-selected on the basis of their purities studied by X-ray diffraction (XRD and chemical analysis. Prepared compositions of glasses precursors were two different theoretical leucite (KAlSi₂O₆ /Bioglass 45S5 (L/Bg ratios. Transformations of raw materials mixtures and glass precursors were studied by differential thermal analyses. On the basis of thermal analysis results, glass ceramics were produced and characterized by XRD. Glass-ceramics were composed of two major crystalline phases, leucite and sodium calcium silicate. Bioactivity tests were performed submerging the glass-ceramics into simulated body fluid (SBF for different periods (1, 5 and 10 days. Bioactive behavior was monitored by XRD and scanning electron microscopy (SEM. Studied samples were found to be bioactive, in which hydroxyapatite layer was developed within 5 days of contact with SBF.

  12. Bioactive glasses and glass-ceramics

    Directory of Open Access Journals (Sweden)

    de Aza, P. N.

    2007-04-01

    Full Text Available Since the late 1960´s, a great interest in the use of bioceramic materials for biomedical applications has been developed. In a previous paper, the authors reviewed crystalline bioceramic materials “sensus stricto”, it is to say, those ceramic materials, constituted for non-metallic inorganic compounds, crystallines and consolidates by thermal treatment of powders at high temperature. In the present review, the authors deal with those called bioactive glasses and glassceramics. Although all of them are also obtained by thermal treatment at high temperature, the first are amorphous and the second are obtained by devitrification of a glass, although the vitreous phase normally prevails on the crystalline phases. After an introduction to the concept of bioactive materials, a short historical review of the bioactive glasses development is made. Its preparation, reactivity in physiological media, mechanism of bonding to living tissues and mechanical strength of the bone-implant interface is also reported. Next, the concept of glass-ceramic and the way of its preparation are exposed. The composition, physicochemical properties and biological behaviour of the principal types of bioactive glasses and glass-ceramic materials: Bioglass®, Ceravital®, Cerabone®, Ilmaplant® and Bioverit® are also reviewed. Finally, a short review on the bioactive-glass coatings and bioactive-composites and most common uses of bioactive-glasses and glass-ceramics are carried out too.

    Desde finales de los años sesenta, se ha despertado un gran interés por el uso de los materiales biocerámicos para aplicaciones biomédicas. En un trabajo previo, los autores hicieron una revisión de los denominados materiales biocerámicos cristalinos en sentido estricto, es decir, de aquellos materiales, constituidos por compuestos inorgánicos no metálicos, cristalinos y consolidados mediante tratamientos térmicos a altas temperaturas. En el presente trabajo, los autores

  13. Bioactivity and properties of a dental adhesive functionalized with polyhedral oligomeric silsesquioxanes (POSS) and bioactive glass.

    Science.gov (United States)

    Rizk, Marta; Hohlfeld, Lisa; Thanh, Loan Tao; Biehl, Ralf; Lühmann, Nicole; Mohn, Dirk; Wiegand, Annette

    2017-09-01

    This study aimed to analyze the effect of infiltrating a commercial adhesive with nanosized bioactive glass (BG-Bi) particles or methacryl-functionalized polyhedral oligomeric silsesquioxanes (POSS) on material properties and bioactivity. An acetone-based dental adhesive (Solobond Plus adhesive, VOCO GmbH, Cuxhaven, Germany) was infiltrated with nanosized bioactive glass particles (0.1 or 1wt%), or with monofunctional or multifunctional POSS particles (10 or 20wt%). Unfilled adhesive served as control. Dispersion and hydrodynamic radius of the nanoparticles were studied by dynamic light scattering. Set specimens were immersed for 28days in artificial saliva at 37°C, and surfaces were mapped for the formation of calcium phospate (Ca/P) precipitates (scanning electron microscopy/energy-dispersive X-ray spectroscopy). Viscosity (rheometry) and the structural characteristic of the networks were studied, such as degree of conversion (FTIR spectroscopy), sol fraction and water sorption. POSS particles showed a good dispersion of the particles for both types of particles being smaller than 3nm, while the bioactive glass particles had a strong tendency to agglomerate. All nanoparticles induced the formation of Ca/P precipitates. The viscosity of the adhesive was not or only slightly increased by POSS particle addition but strongly increased by the bioactive glass particles. The degree of conversion, water sorption and sol fraction showed a maintained or improved network structure and properties when filled with BG-Bi and multifunctional POSS, however, less polymerization was found when loading a monofunctional POSS. Multifunctional POSS may be incorporated into dental adhesives to provide a bioactive potential without changing material properties adversely. Copyright © 2017 The Academy of Dental Materials. Published by Elsevier Ltd. All rights reserved.

  14. Bioactive glass coupling with natural polyphenols: Surface modification, bioactivity and anti-oxidant ability

    Energy Technology Data Exchange (ETDEWEB)

    Cazzola, Martina [Politecnico di Torino, Department of Applied Science and Technology, Institute of Materials Physics and Engineering, C.so Duca degli Abruzzi 24, Torino 10129 (Italy); Corazzari, Ingrid [Università degli Studi di Torino, Department of Chemistry, Via Pietro Giuria 7, Torino 10125 (Italy); Centro Interdipartimentale “G. Scansetti” per lo studio degli amianti e di altri particolati nocivi, Via Pietro Giuria 9, 10125 Torino (Italy); Prenesti, Enrico [Università degli Studi di Torino, Department of Chemistry, Via Pietro Giuria 7, Torino 10125 (Italy); Bertone, Elisa [Politecnico di Torino, Department of Applied Science and Technology, Institute of Materials Physics and Engineering, C.so Duca degli Abruzzi 24, Torino 10129 (Italy); Vernè, Enrica, E-mail: enrica.verne@polito.it [Politecnico di Torino, Department of Applied Science and Technology, Institute of Materials Physics and Engineering, C.so Duca degli Abruzzi 24, Torino 10129 (Italy); Ferraris, Sara [Politecnico di Torino, Department of Applied Science and Technology, Institute of Materials Physics and Engineering, C.so Duca degli Abruzzi 24, Torino 10129 (Italy)

    2016-03-30

    Graphical abstract: - Highlights: • Surface functionalization of bioactive glass with biomolecules has been optimized. • Biomolecules are present and active on the glass surface after functionalization. • Biomolecules affect deposition kinetics and morphology of hydroxyapatite. • Free radical scavenging activity is seen for the first time on bioactive glasses. - Abstract: Polyphenols are actually achieving an increasing interest due to their potential health benefits, such as antioxidant, anticancer, antibacterial and bone stimulation abilities. However their poor bioavailability and stability hamper an effective clinical application as therapeutic principles. The opportunity to couple these biomolecules with synthetic biomaterials, in order to obtain local delivery at the site of interest, improve their bioavailability and stability and combine their properties with the ones of the substrate, is a challenging opportunity for the biomedical research. A silica based bioactive glass, CEL2, has been successfully coupled with gallic acid and natural polyphenols extracted from red grape skins and green tea leaves. The effectiveness of grafting has been verified by means of XPS analyses and the Folin&Ciocalteu tests. In vitro bioactivity has been investigated by soaking in simulated body fluid (SBF). Surface modification after functionalization and early stage reactivity in SBF have been studied by means of zeta potential electrokinetic measurements in KCl and SBF. Finally the antioxidant properties of bare and modified bioactive glasses has been investigated by means of the evaluation of free radical scavenging activity by Electron Paramagnetic Resonance (EPR)/spin trapping technique after UV photolysis of H{sub 2}O{sub 2} highlighting scavenging activity of the bioactive glass.

  15. The Correlation of Pore Size and Bioactivity of Spray-Pyrolyzed Mesoporous Bioactive Glasses

    Directory of Open Access Journals (Sweden)

    Yu-Jen Chou

    2017-05-01

    Full Text Available SiO2–CaO–P2O5-based mesoporous bioactive glasses (MBGs were synthesized by spray pyrolysis in this study. Three commonly used non-ionic tri-block copolymers (L121, P123, and F127 with various lengths of hydrophilic chains were applied as structural templates to achieve different pore sizes. A mesoporous structure was observed in each as-prepared specimen, and the results showed that the L121-treated MBG had the largest pore size. The results of bioactivity tests indicated that the growth of hydroxyapatite is related to the pore size of the materials.

  16. Discovery of Novel Lipid Profiles in PCOS: Do Insulin and Androgen Oppositely Regulate Bioactive Lipid Production?

    Science.gov (United States)

    Li, Shengxian; Chu, Qianqian; Ma, Jing; Sun, Yun; Tao, Tao; Huang, Rong; Liao, Yu; Yue, Jiang; Zheng, Jun; Wang, Lihua; Xue, Xinli; Zhu, Mingjiang; Kang, Xiaonan; Yin, Huiyong; Liu, Wei

    2017-03-01

    Polycystic ovary syndrome (PCOS) is a complex syndrome showing clinical features of an endocrine/metabolic disorder, including hyperinsulinemia and hyperandrogenism. Polyunsaturated fatty acids (PUFAs) and their derivatives, both tightly linked to PCOS and obesity, play important roles in inflammation and reproduction. This study aimed to investigate serum lipid profiles in newly diagnosed patients with PCOS using lipidomics and correlate these features with the hyperinsulinemia and hyperandrogenism associated with PCOS and obesity. Thirty-two newly diagnosed women with PCOS and 34 controls were divided into obese and lean subgroups. A PCOS rat model was used to validate results of the human studies. Serum lipid profiles, including phospholipids, free fatty acids (FFAs), and bioactive lipids, were analyzed using gas chromatography-mass spectrometry (MS) and liquid chromatography-MS. Elevation in phosphatidylcholine and a concomitant decrease in lysophospholipid were found in obese patients with PCOS vs lean controls. Obese patients with PCOS had decreased PUFA levels and increased levels of long-chain saturated fatty acids vs lean controls. Serum bioactive lipids downstream of arachidonic acid were increased in obese controls, but reduced in both obese and lean patients with PCOS vs their respective controls. Patients with PCOS showed abnormal levels of phosphatidylcholine, FFAs, and PUFA metabolites. Circulating insulin and androgens may have opposing effects on lipid profiles in patients with PCOS, particularly on the bioactive lipid metabolites derived from PUFAs. These clinical observations warrant further studies of the molecular mechanisms and clinical implications of PCOS and obesity. Copyright © 2017 by the Endocrine Society

  17. Bioactive Polymeric Composites for Tooth Mineral Regeneration: Physicochemical and Cellular Aspects

    Science.gov (United States)

    Skrtic, Drago; Antonucci, Joseph M.

    2011-01-01

    Our studies of amorphous calcium phosphate (ACP)-based dental materials are focused on the design of bioactive, non-degradable, biocompatible, polymeric composites derived from acrylic monomer systems and ACP by photochemical or chemically activated polymerization. Their intended uses include remineralizing bases/liners, orthodontic adhesives and/or endodontic sealers. The bioactivity of these materials originates from the propensity of ACP, once exposed to oral fluids, to release Ca and PO4 ions (building blocks of tooth and bone mineral) in a sustained manner while spontaneously converting to thermodynamically stable apatite. As a result of ACP's bioactivity, local Ca- and PO4-enriched environments are created with supersaturation conditions favorable for the regeneration of tooth mineral lost to decay or wear. Besides its applicative purpose, our research also seeks to expand the fundamental knowledge base of structure-composition-property relationships existing in these complex systems and identify the mechanisms that govern filler/polymer and composite/tooth interfacial phenomena. In addition to an extensive physicochemical evaluation, we also assess the leachability of the unreacted monomers and in vitro cellular responses to these types of dental materials. The systematic physicochemical and cellular assessments presented in this study typically provide model materials suitable for further animal and/or clinical testing. In addition to their potential dental clinical value, these studies suggest the future development of calcium phosphate-based biomaterials based on composite materials derived from biodegradable polymers and ACP, and designed primarily for general bone tissue regeneration. PMID:22102967

  18. Nutrients, phytochemicals and bioactivity of wild Roman chamomile: a comparison between the herb and its preparations.

    Science.gov (United States)

    Guimarães, Rafaela; Barros, Lillian; Dueñas, Montserrat; Calhelha, Ricardo C; Carvalho, Ana Maria; Santos-Buelga, Celestino; Queiroz, Maria João R P; Ferreira, Isabel C F R

    2013-01-15

    Roman chamomile, Chamaemelum nobile L. (Asteraceae), has been used for medicinal applications, mainly through oral dosage forms (decoctions and infusions). Herein, the nutritional characterisation of C. nobile was performed, and herbal material and its decoction and infusion were submitted to an analysis of phytochemicals and bioactivity evaluation. The antioxidant activity was determined by free radicals scavenging activity, reducing power and inhibition of lipid peroxidation, the antitumour potential was tested in human tumour cell lines (breast, lung, colon, cervical and hepatocellular carcinomas), and the hepatotoxicity was evaluated using a porcine liver primary cell culture. C. nobile proved to be an equilibrated valuable herb rich in carbohydrates and proteins, and poor in fat, providing tocopherols, carotenoids and essential fatty acids (C18:2n6 and C18:3n3). Moreover, the herb and its infusion are a source of phenolic compounds (flavonoids such as flavonols and flavones, phenolic acids and derivatives) and organic acids (oxalic, quinic, malic, citric and fumaric acids) that showed antioxidant and antitumour activities, without hepatotoxicity. The most abundant compounds in the plant extract and infusion were 5-O-caffeoylquinic acid and an apigenin derivative. These, as well as other bioactive compounds, are affected in C. nobile decoction, leading to a lower antioxidant potential and absence of antitumour potential. The plant bioactivity could be explored in the medicine, food, and cosmetic industries. Copyright © 2012 Elsevier Ltd. All rights reserved.

  19. Alkali-free bioactive glasses for bone regeneration

    OpenAIRE

    Kapoor, Saurabh

    2014-01-01

    Bioactive glasses and glass-ceramics are a class of third generation biomaterials which elicit a special response on their surface when in contact with biological fluids, leading to strong bonding to living tissues. The purpose of the present study was to develop diopside based alkali-free bioactive glasses in order to achieve good sintering behaviour, high bioactivity, and a dissolution/ degradation rates compatible with the target applications in bone regeneration and tiss...

  20. Hierarchically Nanoporous Bioactive Glasses for High Efficiency Immobilization of Enzymes

    DEFF Research Database (Denmark)

    He, W.; Min, D.D.; Zhang, X.D.

    2014-01-01

    Bioactive glasses with hierarchical nanoporosity and structures have been heavily involved in immobilization of enzymes. Because of meticulous design and ingenious hierarchical nanostructuration of porosities from yeast cell biotemplates, hierarchically nanostructured porous bioactive glasses can...... and products of catalytic reactions can freely diffuse through open mesopores (2–40 nm). The formation mechanism of hierarchically structured porous bioactive glasses, the immobilization mechanism of enzyme and the catalysis mechanism of immobilized enzyme are then discussed. The novel nanostructure...

  1. Bactericidal effects of bioactive glasses on clinically important aerobic bacteria.

    Science.gov (United States)

    Munukka, Eveliina; Leppäranta, Outi; Korkeamäki, Mika; Vaahtio, Minna; Peltola, Timo; Zhang, Di; Hupa, Leena; Ylänen, Heimo; Salonen, Jukka I; Viljanen, Matti K; Eerola, Erkki

    2008-01-01

    Bioactive glasses (BAGs) have been studied for decades for clinical use, and they have found many dental and orthopedic applications. BAGs have also been shown to have an antibacterial effect e.g., on some oral microorganisms. In this extensive work we show that six powdered BAGs and two sol-gel derived materials have a clear antibacterial effect on 29 clinically important bacterial species. We also incorporated a rapid and accurate flow cytometric (FCM) method to calculate and standardize the numbers of viable bacteria inoculated in the suspensions used in the tests for antibacterial activity. In all materials tested growth inhibition could be demonstrated, although the concentration and time needed for the effect varied depending on the BAG. The most effective glass was S53P4, which had a clear growth-inhibitory effect on all pathogens tested. The sol-gel derived materials CaPSiO and CaPSiO II also showed a strong antibacterial effect. In summary, BAGs were found to clearly inhibit the growth of a wide selection of bacterial species causing e.g., infections on the surfaces of prostheses in the body after implantation.

  2. Bioactive and wood-associated stilbenes as multifunctional antimicrobial and health promoting agents - BIOSTIMUL

    Energy Technology Data Exchange (ETDEWEB)

    Wright, A. von (Univ. of Eastern Finland, Kuopio (Finland). Dept. of Biosciences.), Email: atte.vonWright@uef.fi

    2010-10-15

    Plant polyphenolics have a wide range of bioactivities. Coniferous trees are a rich source of stilbenes, such as pinosylvin in the genus Pinus. Pinosylvin is structurally very similar to resveratrol, a stilbene found in grapes and red berries, and which is reported to have beneficial health effects such as prevention of cardiovascular diseases, tumourigenesis, and according to recent findings, also type II diabetes. In our previous studies the bioactivities of pinosylvin (antimicrobial effects and cytotoxic activities against cancer cells) were very similar to those of resveratrol. In this project we elucidate the potential of pinosylvin and its derivatives in food applications as multifunctional antimicrobial agents with positive health effects (including prevention of type II diabetes) highlighting results. (orig.)

  3. Bioactive and wood-associated stilbenes as multifunctional antimicrobial and health promoting agents - BIOSTIMUL

    Energy Technology Data Exchange (ETDEWEB)

    Wright, A. von (Univ. of Kuopio, Dept. of Biosciences (Finland)), email: atte.vonWright@uku.fi

    2009-10-15

    Plant polyphenolics have a wide range of bioactivities. Coniferous trees are a rich source of stilbenes, such as pinosylvin in the genus Pinus. Pinosylvin is structurally very similar to resveratrol, a stilbene found in grapes and red berries, and which is reported to have beneficial health effects such as prevention of cardiovascular diseases, tumourigenesis, and according to recent findings, also type 2 diabetes. In our previous studies the bioactivities of pinosylvin (antimicrobial effects and cytotoxic activities against cancer cells) were very similar to those of resveratrol. In this project we elucidate the potential of pinosylvin and its derivatives in food applications as multifunctional antimicrobial agents with positive health effects (including prevention of type 2 diabetes) highlighting results. (orig.)

  4. Bioactive and wood-associated stilbenes as multifunctional antimicrobial and health promoting agents (BIOSTIMUL)

    Energy Technology Data Exchange (ETDEWEB)

    Wright, A. von (Kuopio Univ., Department of Biosciences (Finland))

    2008-07-01

    Plant polyphenolics have a wide range of bioactivities. Coniferous trees are a rich source of stilbenes, such as pinosylvin in the genus Pinus. Pinosylvin is structurally very similar to resveratrol, a stilbene found in grapes and red berries, and which is reported to have beneficial health effects such as prevention of cardiovascular diseases, tumourigenesis, and according to recent findings, also type II diabetes. In our previous studies the bioactivities of pinosylvin (antimicrobial effects and cytotoxic activities against cancer cells) were very similar to those of resveratrol. In this project we elucidate the potential of pinosylvin and as derivatives in food applications as multifunctional antimicrobial agents with positive health effects (including prevention of type II diabetes) highlighting results. (orig.)

  5. Effects of an onion by-product on bioactivity and safety markers in healthy rats

    DEFF Research Database (Denmark)

    Roldan-Marin, Eduvigis; Krath, Britta; Poulsen, Morten

    2009-01-01

    Onions are excellent sources of bioactive compounds including fructo-oligosaccharides (FOS) and polyphenols. An onion by-product was characterised in order to be developed as a potentially bioactive food ingredient. Our main aim was to investigate whether the potential health and safety effects...... of this onion by-product were shared by either of two derived fractions, an extract containing the onion FOS and polyphenols and a residue fraction containing mainly cell wall materials. We report here on the effects of feeding these products on markers of potential toxicity, protective enzymes and gut...... environment in healthy rats. Rats were fed during 4 weeks with a diet containing the products or a control feed balanced in carbohydrate. The onion by-product and the extract caused anaemia as expected in rodents for Allium products. No other toxicity was observed, including genotoxicity. Glutathione...

  6. Lactobacillus acidophilus Metabolizes Dietary Plant Glucosides and Externalizes Their Bioactive Phytochemicals

    DEFF Research Database (Denmark)

    Theilmann, Mia Christine; Goh, Yong Jun; Nielsen, Kristian Fog

    2017-01-01

    Therapeutically active glycosylated phytochemicals are ubiquitous in the human diet. The human gut microbiota (HGM) modulates the bioactivities of these compounds, which consequently affect host physiology and microbiota composition. Despite a significant impact on human health, the key players...... of the loci to distinct groups of PGs. Following intracellular deglucosylation, the aglycones of PGs are externalized, rendering them available for absorption by the host or for further modification by other microbiota taxa. The PG utilization loci are conserved in L. acidophilus and closely related...... active plant-derived compounds are widely present in berries, fruits, nuts, and beverages like tea and wine. The bioactivity and bioavailability of these compounds, which are typically glycosylated, are altered by microbial bioconversions in the human gut. Remarkably, little is known about...

  7. Discovery and characterization of novel bioactive peptides from marine secondary products

    DEFF Research Database (Denmark)

    Falkenberg, Susan Skanderup

    antioxidative, antihypertensive, antimicrobial, immunomodulatory, anticancer and diabetes 2 effects among others. However, majority of the research has been focusing on the peptides derived from hydrolysis with commercial industrial enzymes and the usefulness of these hydrolysates.It could be interesting...... whether digestion of fish secondary tissue with gastrointestinal proteases generates peptides, which also have these health promoting properties either in relation to gastrointestinal digestion or as an alternative to the use of industrial proteases. Furthermore, as a bioactive defense system against...... the bacterial load in the water, fish is expected to possess bio-components as small peptides. It could therefore be relevant whether these naturally occurring peptides exhibit other functional and health promoting bioactive properties.On this background the overall goal of the present PhD research...

  8. Marine Bioactives as Functional Food Ingredients: Potential to Reduce the Incidence of Chronic Diseases

    Science.gov (United States)

    Lordan, Sinéad; Ross, R. Paul; Stanton, Catherine

    2011-01-01

    The marine environment represents a relatively untapped source of functional ingredients that can be applied to various aspects of food processing, storage, and fortification. Moreover, numerous marine-based compounds have been identified as having diverse biological activities, with some reported to interfere with the pathogenesis of diseases. Bioactive peptides isolated from fish protein hydrolysates as well as algal fucans, galactans and alginates have been shown to possess anticoagulant, anticancer and hypocholesterolemic activities. Additionally, fish oils and marine bacteria are excellent sources of omega-3 fatty acids, while crustaceans and seaweeds contain powerful antioxidants such as carotenoids and phenolic compounds. On the basis of their bioactive properties, this review focuses on the potential use of marine-derived compounds as functional food ingredients for health maintenance and the prevention of chronic diseases. PMID:21747748

  9. Marine Bioactives as Functional Food Ingredients: Potential to Reduce the Incidence of Chronic Diseases

    Directory of Open Access Journals (Sweden)

    Catherine Stanton

    2011-06-01

    Full Text Available The marine environment represents a relatively untapped source of functional ingredients that can be applied to various aspects of food processing, storage, and fortification. Moreover, numerous marine-based compounds have been identified as having diverse biological activities, with some reported to interfere with the pathogenesis of diseases. Bioactive peptides isolated from fish protein hydrolysates as well as algal fucans, galactans and alginates have been shown to possess anticoagulant, anticancer and hypocholesterolemic activities. Additionally, fish oils and marine bacteria are excellent sources of omega-3 fatty acids, while crustaceans and seaweeds contain powerful antioxidants such as carotenoids and phenolic compounds. On the basis of their bioactive properties, this review focuses on the potential use of marine-derived compounds as functional food ingredients for health maintenance and the prevention of chronic diseases.

  10. Bioactive Peptides from Muscle Sources: Meat and Fish

    Directory of Open Access Journals (Sweden)

    Catherine Stanton

    2011-08-01

    Full Text Available Bioactive peptides have been identified in a range of foods, including plant, milk and muscle, e.g., beef, chicken, pork and fish muscle proteins. Bioactive peptides from food proteins offer major potential for incorporation into functional foods and nutraceuticals. The aim of this paper is to present an outline of the bioactive peptides identified in the muscle protein of meat to date, with a focus on muscle protein from domestic animals and fish. The majority of research on bioactives from meat sources has focused on angiotensin-1-converting enzyme (ACE inhibitory and antioxidant peptides.

  11. StraPep: a structure database of bioactive peptides

    Science.gov (United States)

    Wang, Jian; Yin, Tailang; Xiao, Xuwen; He, Dan; Xue, Zhidong; Jiang, Xinnong; Wang, Yan

    2018-01-01

    Abstract Bioactive peptides, with a variety of biological activities and wide distribution in nature, have attracted great research interest in biological and medical fields, especially in pharmaceutical industry. The structural information of bioactive peptide is important for the development of peptide-based drugs. Many databases have been developed cataloguing bioactive peptides. However, to our knowledge, database dedicated to collect all the bioactive peptides with known structure is not available yet. Thus, we developed StraPep, a structure database of bioactive peptides. StraPep holds 3791 bioactive peptide structures, which belong to 1312 unique bioactive peptide sequences. About 905 out of 1312 (68%) bioactive peptides in StraPep contain disulfide bonds, which is significantly higher than that (21%) of PDB. Interestingly, 150 out of 616 (24%) bioactive peptides with three or more disulfide bonds form a structural motif known as cystine knot, which confers considerable structural stability on proteins and is an attractive scaffold for drug design. Detailed information of each peptide, including the experimental structure, the location of disulfide bonds, secondary structure, classification, post-translational modification and so on, has been provided. A wide range of user-friendly tools, such as browsing, sequence and structure-based searching and so on, has been incorporated into StraPep. We hope that this database will be helpful for the research community. Database URL: http://isyslab.info/StraPep PMID:29688386

  12. Fruit and cereal bioactives: sources, chemistry, and applications

    National Research Council Canada - National Science Library

    Tokusoglu, Ozlem; Hall, Clifford, III

    2011-01-01

    .... It provides detailed information on both beneficial bioactives such as phenolics, flavonoids, tocols, carotenoids, phytosterols, and avenanthramides and toxicant compounds including mycotoxins...

  13. Bioactivity of flours of seeds of leguminous crops Pisum sativum ...

    African Journals Online (AJOL)

    Bioactivity of flours of seeds of leguminous crops Pisum sativum, Phaseolus vulgaris and Glycine max used as botanical insecticides against Sitophilus oryzae Linnaeus (Coleoptera: Curculionidae) on sorghum grains.

  14. Bioactive and inert dental glass-ceramics.

    Science.gov (United States)

    Montazerian, Maziar; Zanotto, Edgar Dutra

    2017-02-01

    The global market for dental materials is predicted to exceed 10 billion dollars by 2020. The main drivers for this growth are easing the workflow of dentists and increasing the comfort of patients. Therefore, remarkable research projects have been conducted and are currently underway to develop improved or new dental materials with enhanced properties or that can be processed using advanced technologies, such as CAD/CAM or 3D printing. Among these materials, zirconia, glass or polymer-infiltrated ceramics, and glass-ceramics (GCs) are of great importance. Dental glass-ceramics are highly attractive because they are easy to process and have outstanding esthetics, translucency, low thermal conductivity, high strength, chemical durability, biocompatibility, wear resistance, and hardness similar to that of natural teeth, and, in certain cases, these materials are bioactive. In this review article, we divide dental GCs into the following two groups: restorative and bioactive. Most restorative dental glass-ceramics (RDGCs) are inert and biocompatible and are used in the restoration and reconstruction of teeth. Bioactive dental glass-ceramics (BDGCs) display bone-bonding ability and stimulate positive biological reactions at the material/tissue interface. BDGCs are suggested for dentin hypersensitivity treatment, implant coating, bone regeneration and periodontal therapy. Throughout this paper, we elaborate on the history, processing, properties and applications of RDGCs and BDGCs. We also report on selected papers that address promising types of dental glass-ceramics. Finally, we include trends and guidance on relevant open issues and research possibilities. © 2016 Wiley Periodicals, Inc. J Biomed Mater Res Part A: 105A: 619-639, 2017. © 2016 Wiley Periodicals, Inc.

  15. Bioactive compounds: historical perspectives, opportunities, and challenges.

    Science.gov (United States)

    Patil, Bhimanagouda S; Jayaprakasha, G K; Chidambara Murthy, K N; Vikram, Amit

    2009-09-23

    Mom's conventional wisdom of eating fruits and vegetables to lead a healthy life has evolved with scientific, fact-finding research during the past four decades due to advances in science of "Foods for Health". Epidemiological and prospective studies have demonstrated the vital role of fruits, vegetables, and nuts in reducing the risk of cancer and cardiovascular diseases. In recent years, several meta-analyses strongly suggested that by adding one serving of fruits and vegetables to daily diet, the risk of cardiovascular diseases will be decreased up to 7%. The multidisciplinary and partnership efforts of agriculture and medical scientists across the globe stimulated interest in establishing certain interdisciplinary centers and institutes focusing on "Foods for Health". While the consumption of various healthy foods continues, several questions about toxicity, bioavailability, and food-drug interactions of bioactive compounds are yet to be fully understood on the basis of scientific evidence. Recent research on elucidation of the molecular mechanisms to understand the "proof of the concept" will provide the perfect answer when consumers are ready for a "consumer-to-farm" rather than the current "farm-to-consumer" approach. The multidisciplinary research and educational efforts will address the role of healthy foods to improve eye, brain, and heart health while reducing the risk of cancer. Through this connection, this review is an attempt to provide insight and historical perspectives on some of the bioactive compounds from the day of discovery to their current status. The bioactive compounds discussed in this review are flavonoids, carotenoids, curcumin, ascorbic acid, and citrus limonoids.

  16. In vitro bioactivity and mechanical properties of bioactive glass nanoparticles/polycaprolactone composites.

    Science.gov (United States)

    Ji, Lijun; Wang, Wenjun; Jin, Duo; Zhou, Songtao; Song, Xiaoli

    2015-01-01

    Nanoparticles of bioactive glass (NBG) with a diameter of 50-90 nm were synthesized using the Stöber method. NBG/PCL composites with different NBG contents (0 wt.%, 10 wt.%, 20 wt.%, 30 wt.% and 40 wt.%) were prepared by a melt blending and thermal injection moulding technique, and characterized with XRD, FTIR, and SEM to study the effect of NBG on the mechanical properties and in vitro bioactivity of the NBG/PCL composites. In spite of the high addition up to 40 wt.%, the NBG could be dispersed homogeneously in the PCL matrix. The elastic modulus of the NBG/PCL composites was improved remarkably from 198±13 MPa to 851±43 MPa, meanwhile the tensile strength was retained in the range of 19-21.5 MPa. The hydrophilic property and degradation behavior of the NBG/PCL composites were also improved with the addition of the NBG. Moreover, the composites with high NBG content showed outstanding in vitro bioactivity after being immersed in simulated body fluid, which could be attributed to the excellent bioactivity of the synthesized NBG. Copyright © 2014. Published by Elsevier B.V.

  17. Physicochemical properties and bioactivity of freeze-cast chitosan nanocomposite scaffolds reinforced with bioactive glass.

    Science.gov (United States)

    Pourhaghgouy, Masoud; Zamanian, Ali; Shahrezaee, Mostafa; Masouleh, Milad Pourbaghi

    2016-01-01

    Chitosan based nanocomposite scaffolds were prepared by freeze casting method through blending constant chitosan concentration with different portions of synthesized bioactive glass nanoparticles (BGNPs). Transmission Electron Microscopy (TEM) image showed that the particles size of bioactive glass (64SiO2.28CaO.8P2O5) prepared by sol-gel method was approximately less than 20 nm. Fourier Transform Infrared Spectroscopy (FT-IR) and X-ray Diffraction (XRD) analysis showed proper interfacial bonding between BGNPs and chitosan polymers. Scanning Electron Microscopy (SEM) images depicted a unidirectional structure with homogenous distribution of BGNPs among chitosan matrix associated with the absence of pure chitosan scaffold's wall pores after addition of only 10 wt.% BGNPs. As the BGNP content increased from 0 to 50 wt.%, the compressive strength and compressive module values increased from 0.034 to 0.419 MPa and 0.41 to 10.77 MPa, respectively. Biodegradation study showed that increase in BGNP content leads to growth of weight loss amount. The in vitro biomineralization studies confirmed the bioactive nature of all nanocomposites. Amount of 30 wt.% BGNPs represented the best concentration for absorption capacity and bioactivity behaviors. Copyright © 2015. Published by Elsevier B.V.

  18. Influence of barium substitution on bioactivity, thermal and physico-mechanical properties of bioactive glass.

    Science.gov (United States)

    Arepalli, Sampath Kumar; Tripathi, Himanshu; Vyas, Vikash Kumar; Jain, Shubham; Suman, Shyam Kumar; Pyare, Ram; Singh, S P

    2015-04-01

    Barium with low concentration in the glasses acts as a muscle stimulant and is found in human teeth. We have made a primary study by substituting barium in the bioactive glass. The chemical composition containing (46.1-X) SiO2--24.3 Na2O-26.9 CaO-2.6 P2O5, where X=0, 0.4, 0.8, 1.2 and 1.6mol% of BaO was chosen and melted in an electric furnace at 1400±5°C. The glasses were characterized to determine their use in biomedical applications. The nucleation and crystallization regimes were determined by DTA and the controlled crystallization was carried out by suitable heat treatment. The crystalline phase formed was identified by using XRD technique. Bioactivity of these glasses was assessed by immersion in simulated body fluid (SBF) for various time periods. The formation of hydroxy carbonate apatite (HCA) layer was identified by FTIR spectrometry, scanning electron microscope (SEM) and XRD which showed the presence of HCA as the main phase in all tested bioactive glass samples. Flexural strength and densities of bioactive glasses have been measured and found to increase with increasing the barium content. The human blood compatibility of the samples was evaluated and found to be pertinent. Copyright © 2015 Elsevier B.V. All rights reserved.

  19. Bioactive glass coupling with natural polyphenols: Surface modification, bioactivity and anti-oxidant ability

    Science.gov (United States)

    Cazzola, Martina; Corazzari, Ingrid; Prenesti, Enrico; Bertone, Elisa; Vernè, Enrica; Ferraris, Sara

    2016-03-01

    Polyphenols are actually achieving an increasing interest due to their potential health benefits, such as antioxidant, anticancer, antibacterial and bone stimulation abilities. However their poor bioavailability and stability hamper an effective clinical application as therapeutic principles. The opportunity to couple these biomolecules with synthetic biomaterials, in order to obtain local delivery at the site of interest, improve their bioavailability and stability and combine their properties with the ones of the substrate, is a challenging opportunity for the biomedical research. A silica based bioactive glass, CEL2, has been successfully coupled with gallic acid and natural polyphenols extracted from red grape skins and green tea leaves. The effectiveness of grafting has been verified by means of XPS analyses and the Folin&Ciocalteu tests. In vitro bioactivity has been investigated by soaking in simulated body fluid (SBF). Surface modification after functionalization and early stage reactivity in SBF have been studied by means of zeta potential electrokinetic measurements in KCl and SBF. Finally the antioxidant properties of bare and modified bioactive glasses has been investigated by means of the evaluation of free radical scavenging activity by Electron Paramagnetic Resonance (EPR)/spin trapping technique after UV photolysis of H2O2 highlighting scavenging activity of the bioactive glass.

  20. Marine Nucleosides: Structure, Bioactivity, Synthesis and Biosynthesis

    Directory of Open Access Journals (Sweden)

    Ri-Ming Huang

    2014-12-01

    Full Text Available Nucleosides are glycosylamines that structurally form part of nucleotide molecules, the building block of DNA and RNA. Both nucleosides and nucleotides are vital components of all living cells and involved in several key biological processes. Some of these nucleosides have been obtained from a variety of marine resources. Because of the biological importance of these compounds, this review covers 68 marine originated nucleosides and their synthetic analogs published up to June 2014. The review will focus on the structures, bioactivities, synthesis and biosynthetic processes of these compounds.

  1. Composite bone cements loaded with a bioactive and ferrimagnetic glass-ceramic: Leaching, bioactivity and cytocompatibility

    International Nuclear Information System (INIS)

    Verné, Enrica; Bruno, Matteo; Miola, Marta; Maina, Giovanni; Bianco, Carlotta; Cochis, Andrea; Rimondini, Lia

    2015-01-01

    In this work, composite bone cements, based on a commercial polymethylmethacrylate matrix (Palamed®) loaded with ferrimagnetic bioactive glass-ceramic particles (SC45), were produced and characterized in vitro. The ferrimagnetic bioactive glass-ceramic belongs to the system SiO 2 –Na 2 O–CaO–P 2 O 5 –FeO–Fe 2 O 3 and contains magnetite (Fe 3 O 4 ) crystals into a residual amorphous bioactive phase. Three different formulations (containing 10, 15 and 20 wt.% of glass-ceramic particles respectively) have been investigated. These materials are intended to be applied as bone fillers for the hyperthermic treatment of bone tumors. The morphological, compositional, calorimetric and mechanical properties of each formulation have been already discussed in a previous paper. The in vitro properties of the composite bone cements described in the present paper are related to iron ion leaching test (by graphite furnace atomic absorption spectrometer), bioactivity (i.e. the ability to stimulate the formation of a hydroxyapatite – HAp – layer on their surface after soaking in simulated body fluid SBF) and cytocompatibility toward human osteosarcoma cells (ATCC CRL-1427, Mg63). Morphological and chemical characterizations by scanning electron microscopy and energy dispersion spectrometry have been performed on the composite samples after each test. The iron release was negligible and all the tested samples showed the growth of HAp on their surface after 28 days of immersion in a simulated body fluid (SBF). Cells showed good viability, morphology, adhesion, density and the ability to develop bridge-like structures on all investigated samples. A synergistic effect between bioactivity and cell mineralization was also evidenced. - Highlights: • An in vitro biological characterization was carried out on ferromagnetic and bioactive composite cements. • No release of iron was revealed in the physiological solution. • Bioactivity tests show hydroxyapatite precipitates

  2. Effect of nitrogen and fluorine on mechanical properties and bioactivity in two series of bioactive glasses.

    Science.gov (United States)

    Bachar, Ahmed; Mercier, Cyrille; Tricoteaux, Arnaud; Hampshire, Stuart; Leriche, Anne; Follet, Claudine

    2013-07-01

    Bioactive glasses are able to bond to bone through formation of carbonated hydroxyapatite in body fluids, and fluoride-releasing bioactive glasses are of interest for both orthopaedic and, in particular, dental applications for caries inhibition. However, because of their poor strength their use is restricted to non-load-bearing applications. In order to increase their mechanical properties, doping with nitrogen has been performed on two series of bioactive glasses: series (I) was a "bioglass" composition (without P2O5) within the quaternary system SiO2-Na2O-CaO-Si3N4 and series (II) was a simple substitution of CaF2 for CaO in series (I) glasses keeping the Na:Ca ratio constant. The objective of this work was to evaluate the effect of the variation in nitrogen and fluorine content on the properties of these glasses. The density, glass transition temperature, hardness and elastic modulus all increased linearly with nitrogen content which indicates that the incorporation of nitrogen stiffens the glass network because N is mainly in 3-fold coordination with Si atoms. Fluorine addition significantly decreases the thermal property values but the mechanical properties of these glasses remain unchanged with fluorine. The combination of both nitrogen and fluorine in oxyfluoronitride glasses gives better mechanical properties at much lower melting temperatures since fluorine reduces the melting point, allows higher solubility of nitrogen and does not affect the higher mechanical properties arising from incorporation of nitrogen. The characterization of these N and F substituted bioactive glasses using (29)Si MAS NMR has shown that the increase in rigidity of the glass network can be explained by the formation of SiO3N, SiO2N2 tetrahedra and Q(4) units with extra bridging anions at the expense of Q(3) units. Bioactivity of the glasses was investigated in vitro by examining apatite formation on the surface of glasses treated in acellular simulated body fluid (SBF) with ion

  3. Composite bone cements loaded with a bioactive and ferrimagnetic glass-ceramic: Leaching, bioactivity and cytocompatibility

    Energy Technology Data Exchange (ETDEWEB)

    Verné, Enrica, E-mail: enrica.verne@polito.it [Institute of Materials Physics and Engineering, Applied Science and Technology Department, Politecnico di Torino, C. so Duca degli Abruzzi 24, 10129 Torino (Italy); Bruno, Matteo [Institute of Materials Physics and Engineering, Applied Science and Technology Department, Politecnico di Torino, C. so Duca degli Abruzzi 24, 10129 Torino (Italy); Miola, Marta [Institute of Materials Physics and Engineering, Applied Science and Technology Department, Politecnico di Torino, C. so Duca degli Abruzzi 24, 10129 Torino (Italy); Department of Health Sciences, Università del Piemonte Orientale “Amedeo Avogadro”, Via Solaroli 17, 28100 Novara (Italy); Maina, Giovanni; Bianco, Carlotta [Traumatology Orthopedics and Occupational Medicine Dept., Università di Torino, Via G. Zuretti 29, 10126 Torino (Italy); Cochis, Andrea [Department of Health Sciences, Università del Piemonte Orientale “Amedeo Avogadro”, Via Solaroli 17, 28100 Novara (Italy); Rimondini, Lia [Department of Health Sciences, Università del Piemonte Orientale “Amedeo Avogadro”, Via Solaroli 17, 28100 Novara (Italy); Consorzio Interuniversitario Nazionale per la Scienza e Tecnologia dei Materiali, Via G. Giusti, 9, 50121 Firenze (Italy)

    2015-08-01

    In this work, composite bone cements, based on a commercial polymethylmethacrylate matrix (Palamed®) loaded with ferrimagnetic bioactive glass-ceramic particles (SC45), were produced and characterized in vitro. The ferrimagnetic bioactive glass-ceramic belongs to the system SiO{sub 2}–Na{sub 2}O–CaO–P{sub 2}O{sub 5}–FeO–Fe{sub 2}O{sub 3} and contains magnetite (Fe{sub 3}O{sub 4}) crystals into a residual amorphous bioactive phase. Three different formulations (containing 10, 15 and 20 wt.% of glass-ceramic particles respectively) have been investigated. These materials are intended to be applied as bone fillers for the hyperthermic treatment of bone tumors. The morphological, compositional, calorimetric and mechanical properties of each formulation have been already discussed in a previous paper. The in vitro properties of the composite bone cements described in the present paper are related to iron ion leaching test (by graphite furnace atomic absorption spectrometer), bioactivity (i.e. the ability to stimulate the formation of a hydroxyapatite – HAp – layer on their surface after soaking in simulated body fluid SBF) and cytocompatibility toward human osteosarcoma cells (ATCC CRL-1427, Mg63). Morphological and chemical characterizations by scanning electron microscopy and energy dispersion spectrometry have been performed on the composite samples after each test. The iron release was negligible and all the tested samples showed the growth of HAp on their surface after 28 days of immersion in a simulated body fluid (SBF). Cells showed good viability, morphology, adhesion, density and the ability to develop bridge-like structures on all investigated samples. A synergistic effect between bioactivity and cell mineralization was also evidenced. - Highlights: • An in vitro biological characterization was carried out on ferromagnetic and bioactive composite cements. • No release of iron was revealed in the physiological solution. • Bioactivity tests

  4. Fabrication and bioactivity behavior of HA/bioactive glass composites in the presence of calcium hexaboride

    Energy Technology Data Exchange (ETDEWEB)

    El-Bassyouni, Gehan T.; Beherei, Hanan H. [Biomaterials Dept., National Research Centre (NRC), Dokki, Cairo (Egypt); Mohamed, Khaled R., E-mail: kh_rezk1966@yahoo.com [Biomaterials Dept., National Research Centre (NRC), Dokki, Cairo (Egypt); Kenawy, Sayed H. [Ceramics Dept., National Research Centre (NRC), Dokki, Cairo (Egypt)

    2016-06-01

    In the current study, composites were prepared using both the synthesized nano-sized hydroxyapatite (HA), bioactive glass (BG) powders (obtained by the traditional melt-quenching route) together with the purchased nano-sized calcium hexaboride (CB) with different ratios and were fired at 1250 °C. The structure and composition of the solid reaction products were analyzed using X-ray diffraction (XRD), Fourier transform infrared (FT-IR) spectroscopy; scanning electron microscope (SEM) coupled with energy dispersive spectroscopy (EDS), transmission electron microscope (TEM) techniques and compressive strength. The mechanical testing was to designate the role of the CB in improving the mechanical property of the prepared composites. In vitro bioactivity of the prepared composites was assessed by soaking in the simulated body fluid (SBF) at 37 ± 0.5 °°C for 10 days. The effect of different ratios of the three components (CB, HA & BG) on the bioactivity properties was assessed to explore the possibility of enhancing such property to perform in vitro imitations of in vivo conditions in the future. It can be pointed out that the Si-HA content in the composition showed outstanding in vitro bioactivity than pure hydroxyapatite which could be attributed to the excellent bioactivity of the synthesized composites. - Highlights: • The prepared of nano-composites containing CB, HA and BG powders were achieved. • The addition of CB powder enhanced the compressive strength for all the composites. • The composites containing high BG and CB contents improved formation of bone-like apatite layer.

  5. Composite bone cements loaded with a bioactive and ferrimagnetic glass-ceramic: Leaching, bioactivity and cytocompatibility.

    Science.gov (United States)

    Verné, Enrica; Bruno, Matteo; Miola, Marta; Maina, Giovanni; Bianco, Carlotta; Cochis, Andrea; Rimondini, Lia

    2015-08-01

    In this work, composite bone cements, based on a commercial polymethylmethacrylate matrix (Palamed®) loaded with ferrimagnetic bioactive glass-ceramic particles (SC45), were produced and characterized in vitro. The ferrimagnetic bioactive glass-ceramic belongs to the system SiO2-Na2O-CaO-P2O5-FeO-Fe2O3 and contains magnetite (Fe3O4) crystals into a residual amorphous bioactive phase. Three different formulations (containing 10, 15 and 20 wt.% of glass-ceramic particles respectively) have been investigated. These materials are intended to be applied as bone fillers for the hyperthermic treatment of bone tumors. The morphological, compositional, calorimetric and mechanical properties of each formulation have been already discussed in a previous paper. The in vitro properties of the composite bone cements described in the present paper are related to iron ion leaching test (by graphite furnace atomic absorption spectrometer), bioactivity (i.e. the ability to stimulate the formation of a hydroxyapatite - HAp - layer on their surface after soaking in simulated body fluid SBF) and cytocompatibility toward human osteosarcoma cells (ATCC CRL-1427, Mg63). Morphological and chemical characterizations by scanning electron microscopy and energy dispersion spectrometry have been performed on the composite samples after each test. The iron release was negligible and all the tested samples showed the growth of HAp on their surface after 28 days of immersion in a simulated body fluid (SBF). Cells showed good viability, morphology, adhesion, density and the ability to develop bridge-like structures on all investigated samples. A synergistic effect between bioactivity and cell mineralization was also evidenced. Copyright © 2015 Elsevier B.V. All rights reserved.

  6. Fabrication and bioactivity behavior of HA/bioactive glass composites in the presence of calcium hexaboride

    International Nuclear Information System (INIS)

    El-Bassyouni, Gehan T.; Beherei, Hanan H.; Mohamed, Khaled R.; Kenawy, Sayed H.

    2016-01-01

    In the current study, composites were prepared using both the synthesized nano-sized hydroxyapatite (HA), bioactive glass (BG) powders (obtained by the traditional melt-quenching route) together with the purchased nano-sized calcium hexaboride (CB) with different ratios and were fired at 1250 °C. The structure and composition of the solid reaction products were analyzed using X-ray diffraction (XRD), Fourier transform infrared (FT-IR) spectroscopy; scanning electron microscope (SEM) coupled with energy dispersive spectroscopy (EDS), transmission electron microscope (TEM) techniques and compressive strength. The mechanical testing was to designate the role of the CB in improving the mechanical property of the prepared composites. In vitro bioactivity of the prepared composites was assessed by soaking in the simulated body fluid (SBF) at 37 ± 0.5 °°C for 10 days. The effect of different ratios of the three components (CB, HA & BG) on the bioactivity properties was assessed to explore the possibility of enhancing such property to perform in vitro imitations of in vivo conditions in the future. It can be pointed out that the Si-HA content in the composition showed outstanding in vitro bioactivity than pure hydroxyapatite which could be attributed to the excellent bioactivity of the synthesized composites. - Highlights: • The prepared of nano-composites containing CB, HA and BG powders were achieved. • The addition of CB powder enhanced the compressive strength for all the composites. • The composites containing high BG and CB contents improved formation of bone-like apatite layer.

  7. Bioactive Polymeric Materials for Tissue Repair

    Directory of Open Access Journals (Sweden)

    Diane R. Bienek

    2017-01-01

    Full Text Available Bioactive polymeric materials based on calcium phosphates have tremendous appeal for hard tissue repair because of their well-documented biocompatibility. Amorphous calcium phosphate (ACP-based ones additionally protect against unwanted demineralization and actively support regeneration of hard tissue minerals. Our group has been investigating the structure/composition/property relationships of ACP polymeric composites for the last two decades. Here, we present ACP’s dispersion in a polymer matrix and the fine-tuning of the resin affects the physicochemical, mechanical, and biological properties of ACP polymeric composites. These studies illustrate how the filler/resin interface and monomer/polymer molecular structure affect the material’s critical properties, such as ion release and mechanical strength. We also present evidence of the remineralization efficacy of ACP composites when exposed to accelerated acidic challenges representative of oral environment conditions. The utility of ACP has recently been extended to include airbrushing as a platform technology for fabrication of nanofiber scaffolds. These studies, focused on assessing the feasibility of incorporating ACP into various polymer fibers, also included the release kinetics of bioactive calcium and phosphate ions from nanofibers and evaluate the biorelevance of the polymeric ACP fiber networks. We also discuss the potential for future integration of the existing ACP scaffolds into therapeutic delivery systems used in the precision medicine field.

  8. Angiogenesis stimulated by novel nanoscale bioactive glasses

    International Nuclear Information System (INIS)

    Mao, Cong; Chen, Xiaofeng; Miao, Guohou; Lin, Cai

    2015-01-01

    The ability of biomaterials to induce rapid vascular formation is critical in tissue regeneration. Combining recombinant angiogenic growth factors with bioengineered constructs have proven to be difficult due to several issues, including the instability of recombinant proteins, the need for sustained delivery and the dosage of factors. New formulations of bioactive glass, 58S nanosized bioactive glass (58S-NBG), have been reported to enhance wound healing in animal models better than the first generation of 45S5 Bioglass. Therefore, we investigated the effects of extracts of 58S-NBG and 80S-NBG on cultures of human umbilical vein endothelial cells (HUVECs). Cell viability was assessed by MTS assay. In vitro angiogenesis was measured using an ECM gel tube formation assay, and levels of mRNAs for five angiogenic related genes were measured by qRT-PCR. Extracts of 58S-NBG and 80S-NBG stimulated the proliferation of HUVECs, accelerated cell migration, up-regulated expression of the vascular endothelial growth factor, basic fibroblast growth factor, their receptors, and endothelial nitric oxide synthase, resulting in enhanced tube formation in vitro. The enhanced angiogenic response correlated with increased levels of Ca and Si in the extracts of 58S-NBG and 80S-NBG. The ability of 58S-NBG and 80S-NBG to stimulate angiogenesis in vitro provides alternative approaches for stimulating neovascularization of tissue-engineered constructs. (paper)

  9. Bioactive endophytes warrant intensified exploration and conservation.

    Science.gov (United States)

    Smith, Stephen A; Tank, David C; Boulanger, Lori-Ann; Bascom-Slack, Carol A; Eisenman, Kaury; Kingery, David; Babbs, Beatrice; Fenn, Kathleen; Greene, Joshua S; Hann, Bradley D; Keehner, Jocelyn; Kelley-Swift, Elizabeth G; Kembaiyan, Vivek; Lee, Sun Jin; Li, Puyao; Light, David Y; Lin, Emily H; Ma, Cong; Moore, Emily; Schorn, Michelle A; Vekhter, Daniel; Nunez, Percy V; Strobel, Gary A; Donoghue, Michael J; Strobel, Scott A

    2008-08-25

    A key argument in favor of conserving biodiversity is that as yet undiscovered biodiversity will yield products of great use to humans. However, the link between undiscovered biodiversity and useful products is largely conjectural. Here we provide direct evidence from bioassays of endophytes isolated from tropical plants and bioinformatic analyses that novel biology will indeed yield novel chemistry of potential value. We isolated and cultured 135 endophytic fungi and bacteria from plants collected in Peru. nrDNAs were compared to samples deposited in GenBank to ascertain the genetic novelty of cultured specimens. Ten endophytes were found to be as much as 15-30% different than any sequence in GenBank. Phylogenetic trees, using the most similar sequences in GenBank, were constructed for each endophyte to measure phylogenetic distance. Assays were also conducted on each cultured endophyte to record bioactivity, of which 65 were found to be bioactive. The novelty of our contribution is that we have combined bioinformatic analyses that document the diversity found in environmental samples with culturing and bioassays. These results highlight the hidden hyperdiversity of endophytic fungi and the urgent need to explore and conserve hidden microbial diversity. This study also showcases how undergraduate students can obtain data of great scientific significance.

  10. Bioactive endophytes warrant intensified exploration and conservation.

    Directory of Open Access Journals (Sweden)

    Stephen A Smith

    2008-08-01

    Full Text Available A key argument in favor of conserving biodiversity is that as yet undiscovered biodiversity will yield products of great use to humans. However, the link between undiscovered biodiversity and useful products is largely conjectural. Here we provide direct evidence from bioassays of endophytes isolated from tropical plants and bioinformatic analyses that novel biology will indeed yield novel chemistry of potential value.We isolated and cultured 135 endophytic fungi and bacteria from plants collected in Peru. nrDNAs were compared to samples deposited in GenBank to ascertain the genetic novelty of cultured specimens. Ten endophytes were found to be as much as 15-30% different than any sequence in GenBank. Phylogenetic trees, using the most similar sequences in GenBank, were constructed for each endophyte to measure phylogenetic distance. Assays were also conducted on each cultured endophyte to record bioactivity, of which 65 were found to be bioactive.The novelty of our contribution is that we have combined bioinformatic analyses that document the diversity found in environmental samples with culturing and bioassays. These results highlight the hidden hyperdiversity of endophytic fungi and the urgent need to explore and conserve hidden microbial diversity. This study also showcases how undergraduate students can obtain data of great scientific significance.

  11. Bioactive Peptides in Animal Food Products

    Directory of Open Access Journals (Sweden)

    Marzia Albenzio

    2017-05-01

    Full Text Available Proteins of animal origin represent physiologically active components in the human diet; they exert a direct action or constitute a substrate for enzymatic hydrolysis upon food processing and consumption. Bioactive peptides may descend from the hydrolysis by digestive enzymes, enzymes endogenous to raw food materials, and enzymes from microorganisms added during food processing. Milk proteins have different polymorphisms for each dairy species that influence the amount and the biochemical characteristics (e.g., amino acid chain, phosphorylation, and glycosylation of the protein. Milk from other species alternative to cow has been exploited for their role in children with cow milk allergy and in some infant pathologies, such as epilepsy, by monitoring the immune status. Different mechanisms concur for bioactive peptides generation from meat and meat products, and their functionality and application as functional ingredients have proven effects on consumer health. Animal food proteins are currently the main source of a range of biologically-active peptides which have gained special interest because they may also influence numerous physiological responses in the organism. The addition of probiotics to animal food products represent a strategy for the increase of molecules with health and functional properties.

  12. Preparation of radiolabeled bioactive asbestos fibers

    Energy Technology Data Exchange (ETDEWEB)

    Tewson, T J; Francsechini, M P; Scheule, R K; Holian, A [Texas Univ., Houston, TX (USA). Health Science Center

    1991-01-01

    We have developed an efficient procedure to radiolabel asbestos fibers while retaining the bioactivity of the fibers. The fibers are labeled with {sup 68}Ge. The {sup 68}Ge decays into {sup 68}Ga, which then can be detected by its characteristic positron emission. Both chrysotile and crocidolite asbestos, a serpentine and an amphibole, respectively, were radiolabeled successfully. Mild reaction conditions and short reaction times were found under which {similar to}90% of the added {sup 68}Ge and {sup 68}Ga bound to the fibers. The radiolabel was retained even after washing the fibers extensively with physiologic buffers. The effects of the labeling on the bioactivity of the fibers were evaluated in an in vitro assay using guinea pig alveolar macrophages as a target cell. Labeled chrysotile fibers were found to retain >95% of their ability to stimulate these cells. The labeling procedure described in this study should be useful in preparing labeled fibers to investigate both in vitro and in vivo phenomena. (author).

  13. Bioactivity and chemical ecology of some intertidal animals

    Digital Repository Service at National Institute of Oceanography (India)

    Parulekar, A.H.; Shirwaikar, P.

    stream_size 7 stream_content_type text/plain stream_name Bioactive_Com_Mar_Org_1991_29.pdf.txt stream_source_info Bioactive_Com_Mar_Org_1991_29.pdf.txt Content-Encoding ISO-8859-1 Content-Type text/plain; charset=ISO-8859-1 ...

  14. Abrasive wear behaviour of bio-active glass ceramics containing ...

    Indian Academy of Sciences (India)

    In this study, abrasive wear behaviour of bio-active glass ceramic materials produced with two different processes is studied. Hot pressing process and conventional casting and controlled crystallization process were used to produce bio-active ceramics. Fracture toughness of studied material was calculated by fracture ...

  15. calcium sulphate hemihydrate and bioactive glass composites for ...

    Indian Academy of Sciences (India)

    Home; Journals; Bulletin of Materials Science; Volume 41; Issue 2. In vitro bioactivity evaluation of α -calcium sulphate hemihydrate and bioactive glass composites for their potential use in bone regeneration. YANYAN ZHENG CHENGDONG XIONG DUJUAN ZHANG LIFANG ZHANG. Volume 41 Issue 2 April 2018 Article ID ...

  16. Indication of bioactive candidates among body volatiles of ...

    African Journals Online (AJOL)

    Gregarious adult locusts are believed to release many bioactive volatiles from their bodies for the mediation of their biological characteristics. The determination of these bioactive body volatiles can contribute to the development of new, environmentally benign methods of locust control. An important locust, Locusta ...

  17. Bioactive Peptides in Milk Products. | Tirelli | Journal of Food ...

    African Journals Online (AJOL)

    Some peptides produced in vitro or in vivo by enzymatic hydrolysis of caseins and whey protein can affect some biological functions of the body and therefore they are called bioactive peptides. In this paper the physiological significance of bioactive peptides is reviewed and the analytical methods for their purification and ...

  18. Nutrient reference values for bioactives: new approaches needed?

    DEFF Research Database (Denmark)

    Biesalski, Hans Konrad; Erdman Jr., John W.; Hathcock, John

    2013-01-01

    Nutrients can be classified as either "essential" or "non-essential," the latter are also termed bioactive substances. Whereas the absence of essential nutrients from the diet results in overt deficiency often times with moderate to severe physiological decrements, the absence of bioactive substa...

  19. The ecological dynamics and trajectories of bioactive compounds in ...

    African Journals Online (AJOL)

    Result revealed seven bioactive compounds with anthraquinone totally absent from all the species in the four locations. The seven bioactive compounds were apparently more in the leaves than other parts of the plants. Among the four locations alkaloid, triterpene, glycoside, carbohydrate, flavonoid and tannin were high in ...

  20. Berry Leaves: An Alternative Source of Bioactive Natural Products of Nutritional and Medicinal Value

    Directory of Open Access Journals (Sweden)

    Anastasia-Varvara Ferlemi

    2016-06-01

    Full Text Available Berry fruits are recognized, worldwide, as “superfoods” due to the high content of bioactive natural products and the health benefits deriving from their consumption. Berry leaves are byproducts of berry cultivation; their traditional therapeutic use against several diseases, such as the common cold, inflammation, diabetes, and ocular dysfunction, has been almost forgotten nowadays. Nevertheless, the scientific interest regarding the leaf composition and beneficial properties grows, documenting that berry leaves may be considered an alternative source of bioactives. The main bioactive compounds in berry leaves are similar as in berry fruits, i.e., phenolic acids and esters, flavonols, anthocyanins, and procyanidins. The leaves are one of the richest sources of chlorogenic acid. In various studies, these secondary metabolites have demonstrated antioxidant, anti-inflammatory, cardioprotective, and neuroprotective properties. This review focuses on the phytochemical composition of the leaves of the commonest berry species, i.e., blackcurrant, blackberry, raspberry, bilberry, blueberry, cranberry, and lingonberry leaves, and presents their traditional medicinal uses and their biological activities in vitro and in vivo.

  1. Integrative approach to analyze biodiversity and anti-inflammatory bioactivity of Wedelia medicinal plants.

    Directory of Open Access Journals (Sweden)

    Wen-Ching Lin

    Full Text Available For the development of "medical foods" and/or botanical drugs as defined USA FDA, clear and systemic characterizations of the taxonomy, index phytochemical components, and the functional or medicinal bioactivities of the reputed or candidate medicinal plant are needed. In this study, we used an integrative approach, including macroscopic and microscopic examination, marker gene analysis, and chemical fingerprinting, to authenticate and validate various species/varieties of Wedelia, a reputed medicinal plant that grows naturally and commonly used in Asian countries. The anti-inflammatory bioactivities of Wedelia extracts were then evaluated in a DSS-induced murine colitis model. Different species/varieties of Wedelia exhibited distinguishable morphology and histological structures. Analysis of the ribosomal DNA internal transcribed spacer (ITS region revealed significant differences among these plants. Chemical profiling of test Wedelia species demonstrated candidate index compounds and distinguishable secondary metabolites, such as caffeic acid derivatives, which may serve as phytochemical markers or index for quality control and identification of specific Wedelia species. In assessing their effect on treating DSS induced-murine colitis, we observed that only the phytoextract from W. chinensis species exhibited significant anti-inflammatory bioactivity on DSS-induced murine colitis among the various Wedelia species commonly found in Taiwan. Our results provide a translational research approach that may serve as a useful reference platform for biotechnological applications of traditional phytomedicines. Our findings indicate that specific Wedelia species warrant further investigation for potential treatment of human inflammatory bowel disease.

  2. Bioactive glass-poly (ε-caprolactone) composite scaffolds with 3 dimensionally hierarchical pore networks

    International Nuclear Information System (INIS)

    Yun, Hui-suk; Kim, Seung-eon; Park, Eui Kyun

    2011-01-01

    Hierarchically mesoporous-macroporous-giant-porous bioactive glass/poly ε-caprolactone (PCL) composite scaffolds were prepared using a combination of the sol-gel method, evaporation-induced self-assembly process in the presence of nonionic triblock copolymer, EO 100 PO 65 EO 100 (F127), as template, salt leaching method, and rapid prototyping techniques. F127 acts as a template, inducing the formation of mesopores, NaCl with sizes between 25 and 33 μm provides macro-pores after leaching, and rapid prototyping produces giant-pores. The structure and morphology of the scaffolds were characterized by the field emission scanning electron microscopy, transmission electron microscopy, and Hg porosimetry. The mechanical properties of the scaffolds were examined by the dynamic mechanical analysis. Their in vitro bioactivities were confirmed by immersing the scaffolds in simulated body fluid. Their biocompatibilities were also evaluated by culturing human bone marrow stromal cells on the scaffolds. The scaffolds show good molding capabilities, mechanical properties, 3 dimensionally well-interconnected pore structures, bioactivities, and biocompatibilities in vitro. Depending on the amount of NaCl, the scaffolds also show unique sponge-like properties, but still retain better mechanical properties than general salt leaching derived PCL scaffolds. All of the data provide good evidence that the obtained scaffolds possess excellent potential for applications in the fields of tissue engineering and drug storage.

  3. Corrosion mechanism and bioactivity of borate glasses analogue to Hench’s bioglass

    Directory of Open Access Journals (Sweden)

    Mona A. Ouis

    2012-09-01

    Full Text Available Bioactive borate glasses (from the system Na2O-CaO-B2O3-P2O5 and corresponding glass-ceramics as a new class of scaffold material were prepared by full replacement of SiO2 with B2O3 in Hench patented bioactive glass. The prepared samples were investigated by differential thermal analysis (DTA, Fourier transform infrared (FTIR spectroscopy and X-ray diffraction (XRD analysis. The DTA data were used to find out the proper heat treatment temperatures for preparation of the appropriate glass-ceramics with high crystallinity. The prepared crystalline glass-ceramics derivatives were examined by XRD to identify the crystalline phases that were precipitated during controlled thermal treatment. The FTIR spectroscopy was used to justify the formation of hydroxyapatite as an indication of the bioactivity potential or activity of the studied ternary borate glasses or corresponding glass-ceramics after immersion in aqueous phosphate solution. The corrosion results are interpreted on the basis of suggested recent views on the corrosion mechanism of such modified borate glasses in relation to their composition and constitution.

  4. Investigating the Antimicrobial Bioactivity of Cyano bacterial Extracts on Some Plant and Human Pathogens

    International Nuclear Information System (INIS)

    El-Semary, N.A.; Osman, M.E.; Ahmed, A.S.; Botros, H.W.; Farag, A.T.

    2014-01-01

    The search for broad spectrum antimicrobial agents against microbial pathogens, as the available bioactive compounds, has decreasing efficacy and the multidrug resistance trait is spreading among pathogens. Accordingly, the study was carried out to investigate the antimicrobial bioactivity of extracts derived from a cyano bacterial strain from Egypt. The solvents used were diethyl ether, chloroform and methanol. The antimicrobial bioassay of the lipophilic fraction dissolved in diethyl ether of Synechococcus spp. (isolated from Wadi El-Natroun, Egypt) showed the highest broad spectrum bioactivity as it inhibited the growth of both plant and human pathogens. The extract was also effective on the filamentous plant pathogenic fungi Aspergillus flavus and Aspergillus niger. The effects of incubation periods, growth media and pH values on both growth and antimicrobial activity of Synechococcus spp. were investigated. Chu medium was the medium that gave the highest growth followed by BG11 medium then Oscillatoria medium and all these three media showed antibacterial activities but only BG11 showed both antibacterial and antifungal activities after 18 days of incubation. The pH value 10 proved to be the best for growth and antimicrobial activities of Synechococcus spp. in BG11 medium

  5. Evaluating the potential bioactivity of a novel compound ER1626.

    Science.gov (United States)

    Wang, Lijun; Zeng, Yanyan; Wang, Tianling; Liu, Hongyi; Xiao, Hong; Xiang, Hua

    2014-01-01

    ER1626, a novel compound, is a derivate of indeno-isoquinoline ketone. This study was designed to evaluate the biological activity and potential anti-tumor mechanism of ER1626. MTT assay, scratch assay and flow cytometry were used to determine cell proliferation, cell migration and cell cycle distribution as well as cell apoptosis on human breast cancer MCF-7 cells and endometrial cancer Ishikawa cells. We also explored the antiangiogenic effect of ER1626 on HUVEC cells and chicken embryos. The expression of estrogen receptor protein was investigated with western-blot analysis. ER1626 down-regulated the expression of estrogen receptor α protein and up-regulated β protein in MCF-7 and Ishikawa cells. The value of IC50 of ER1626 on MCF-7 and Ishikawa cells were respectively 8.52 and 3.08 µmol/L. Meanwhile, ER1626 decreased VEGF secretion of MCF-7 and Ishikawa cells, disturbed the formation of VEGF-stimulated tubular structure in HUVEC cells, and inhibited the angiogenesis on the chicken chorioallantoic membrane. Scratch assay revealed that ER1626 suppressed the migration of MCF-7, Ishikawa and HUVEC cells. In addition to induction tumor cell apoptosis, ER1626 arrested cell cycle in G1/G0 phase in MCF-7 cells and G2/M phase in Ishikawa cells. In conclusion, our results demonstrated that ER1626 has favorable bioactivities to be a potential candidate against breast cancer and angiogenesis.

  6. Evaluating the potential bioactivity of a novel compound ER1626.

    Directory of Open Access Journals (Sweden)

    Lijun Wang

    Full Text Available ER1626, a novel compound, is a derivate of indeno-isoquinoline ketone. This study was designed to evaluate the biological activity and potential anti-tumor mechanism of ER1626.MTT assay, scratch assay and flow cytometry were used to determine cell proliferation, cell migration and cell cycle distribution as well as cell apoptosis on human breast cancer MCF-7 cells and endometrial cancer Ishikawa cells. We also explored the antiangiogenic effect of ER1626 on HUVEC cells and chicken embryos. The expression of estrogen receptor protein was investigated with western-blot analysis.ER1626 down-regulated the expression of estrogen receptor α protein and up-regulated β protein in MCF-7 and Ishikawa cells. The value of IC50 of ER1626 on MCF-7 and Ishikawa cells were respectively 8.52 and 3.08 µmol/L. Meanwhile, ER1626 decreased VEGF secretion of MCF-7 and Ishikawa cells, disturbed the formation of VEGF-stimulated tubular structure in HUVEC cells, and inhibited the angiogenesis on the chicken chorioallantoic membrane. Scratch assay revealed that ER1626 suppressed the migration of MCF-7, Ishikawa and HUVEC cells. In addition to induction tumor cell apoptosis, ER1626 arrested cell cycle in G1/G0 phase in MCF-7 cells and G2/M phase in Ishikawa cells.In conclusion, our results demonstrated that ER1626 has favorable bioactivities to be a potential candidate against breast cancer and angiogenesis.

  7. Synthesis of densely functionalized enantiopure indolizidines by ring-closing metathesis (RCM of hydroxylamines from carbohydrate-derived nitrones

    Directory of Open Access Journals (Sweden)

    Goti Andrea

    2007-12-01

    Full Text Available Abstract Background Indolizidine alkaloids widely occur in nature and display interesting biological activity. This is the reason for which their total synthesis as well as the synthesis of non-natural analogues still attracts the attention of many research groups. To establish new straightforward accesses to these molecules is therefore highly desirable. Results The ring closing metathesis (RCM of enantiopure hydroxylamines bearing suitable unsaturated groups cleanly afforded piperidine derivatives in good yields. Further cyclization and deprotection of the hydroxy groups gave novel highly functionalized indolizidines. The synthesis of a pyrroloazepine analogue is also described. Conclusion We have developed a new straightforward methodology for the synthesis of densely functionalized indolizidines and pyrroloazepine analogues in 6 steps and 30–60% overall yields from enantiopure hydroxylamines obtained straightforwardly from carbohydrate-derived nitrones.

  8. Bioactive and Antibacterial Coatings Based on Zein/Bioactive Glass Composites by Electrophoretic Deposition

    Directory of Open Access Journals (Sweden)

    Nima Meyer

    2018-01-01

    Full Text Available This study investigated the electrophoretic deposition (EPD of the natural polymer zein combined with bioactive glass (BG particles. Through the deposition of various BG compositions, namely 45S5 BG and Cu-doped BG, this work sought to demonstrate the ability of the films to potentiate the formation of hydroxyapatite (HA in contact with simulated body fluid (SBF. Following incubation in SBF, the physical and chemical surface properties of the EPD films were evaluated using different characterization techniques. The formation of HA at the surface of the coatings following immersion in SBF was confirmed using Fourier transform infrared spectroscopy (FTIR. The results demonstrated HA formation in all coatings after seven days of immersion in SBF. Coating morphology and degradation of the zein films were characterized using environmental scanning electron microscopy (ESEM. The results confirmed EPD as a very convenient room temperature technique for production of ion releasing, bioactive, and antibacterial coatings for potential application in orthopedics.

  9. Bioactive substances of the Techirghiol therapeutic mud

    Directory of Open Access Journals (Sweden)

    Mihail Hoteteu

    2018-02-01

    Full Text Available The study aims to characterize Techirghiol's sapropelic mud both by determining the organic and inorganic composition of the constituent phases and by isolating some compounds of humic substances. The distribution between the solid and liquid phases of the peloid of the Ca2+, Mg2+, Fe3+cations, PO43- anion, bioactive compounds of the protein, lipid and carbohydrate classes as well as the phosphatase activity of Techirghiol sapropelic mud are analyzed. The mud is fractionated using the pH and solvent polarity variation and is spectrophotometrically characterized based on absorption in the wavelength range 340-700 nm humic acids and fulvic acids differentiated on the basis of solubility and molecular mass.

  10. Bioactive glass coatings for orthopedic metallic implants

    Energy Technology Data Exchange (ETDEWEB)

    Lopez-Esteban, Sonia; Saiz, Eduardo; Fujino, Sigheru; Oku, Takeo; Suganuma, Katsuaki; Tomsia, Antoni P.

    2003-06-30

    The objective of this work is to develop bioactive glass coatings for metallic orthopedic implants. A new family of glasses in the SiO2-Na2O-K2O-CaO-MgO-P2O5 system has been synthesized and characterized. The glass properties (thermal expansion, softening and transformation temperatures, density and hardness) are in line with the predictions of established empirical models. The optimized firing conditions to fabricate coatings on Ti-based and Co-Cr alloys have been determined and related to the glass properties and the interfacial reactions. Excellent adhesion to alloys has been achieved through the formation of 100-200 nm thick interfacial layers (Ti5Si3 on Ti-based alloys and CrOx on Co-Cr). Finally, glass coatings, approximately 100 mu m thick, have been fabricated onto commercial Ti alloy-based dental implants.

  11. Bioactivity and Functionality of Bonghwa Sweetfish

    International Nuclear Information System (INIS)

    Kim, Jae Hun; Lee, Ju Woon; Choi, Jong Il; Song, Beom Seok; Yoon, Yo Han; Sung, Nak Yun; Jeong, Pil Mun

    2010-04-01

    - Smoked sweetfish had higher contents of calories, carbohydrate, protein, fat sodium, and calcium than unsmoked sweetfish - DHA and EPA which are omega-3 fatty acid and have therapeutic effects on arthritis and high blood pressure - Proteins and peptide from sweetfish had various bioactivities such as antioxidation, hypertensive, especially for antiinflammatory, and whitening effects. However no anticancer effect was observed - The proteins and peptide suppressed nitric oxide and cytokines (a-TNF, IL-6, IL-1 beta), and prostaglandin (PGE2) productions, and mRNA related iNOS and cyclooxygenase (COX-2), which are related to inflammation - The proteins and peptide prevented tyrosinase formation, which is related formation of melanin, and also showed preventive effects of melanin synthesis, antioxidation and anti-aging effects. Thus, the proteins and peptides from sweetfish may be useful source for cosmetics

  12. Bioactive Compounds Found in Brazilian Cerrado Fruits.

    Science.gov (United States)

    Bailão, Elisa Flávia Luiz Cardoso; Devilla, Ivano Alessandro; da Conceição, Edemilson Cardoso; Borges, Leonardo Luiz

    2015-10-09

    Functional foods include any natural product that presents health-promoting effects, thereby reducing the risk of chronic diseases. Cerrado fruits are considered a source of bioactive substances, mainly phenolic compounds, making them important functional foods. Despite this, the losses of natural vegetation in the Cerrado are progressive. Hence, the knowledge propagation about the importance of the species found in Cerrado could contribute to the preservation of this biome. This review provides information about Cerrado fruits and highlights the structures and pharmacologic potential of functional compounds found in these fruits. Compounds detected in Caryocar brasiliense Camb. (pequi), Dipteryx alata Vog. (baru), Eugenia dysenterica DC. (cagaita), Eugenia uniflora L. (pitanga), Genipa americana L. (jenipapo), Hancornia speciosa Gomes (mangaba), Mauritia flexuosa L.f. (buriti), Myrciaria cauliflora (DC) Berg (jabuticaba), Psidium guajava L. (goiaba), Psidium spp. (araçá), Solanum lycocarpum St. Hill (lobeira), Spondias mombin L. (cajá), Annona crassiflora Mart. (araticum), among others are reported here.

  13. Bioactivity and Functionality of Bonghwa Sweetfish

    Energy Technology Data Exchange (ETDEWEB)

    Kim, Jae Hun; Lee, Ju Woon; Choi, Jong Il; Song, Beom Seok; Yoon, Yo Han; Sung, Nak Yun; Jeong, Pil Mun

    2010-04-15

    - Smoked sweetfish had higher contents of calories, carbohydrate, protein, fat sodium, and calcium than unsmoked sweetfish - DHA and EPA which are omega-3 fatty acid and have therapeutic effects on arthritis and high blood pressure - Proteins and peptide from sweetfish had various bioactivities such as antioxidation, hypertensive, especially for antiinflammatory, and whitening effects. However no anticancer effect was observed - The proteins and peptide suppressed nitric oxide and cytokines (a-TNF, IL-6, IL-1 beta), and prostaglandin (PGE2) productions, and mRNA related iNOS and cyclooxygenase (COX-2), which are related to inflammation - The proteins and peptide prevented tyrosinase formation, which is related formation of melanin, and also showed preventive effects of melanin synthesis, antioxidation and anti-aging effects. Thus, the proteins and peptides from sweetfish may be useful source for cosmetics

  14. Bioactive Compounds Found in Brazilian Cerrado Fruits

    Directory of Open Access Journals (Sweden)

    Elisa Flávia Luiz Cardoso Bailão

    2015-10-01

    Full Text Available Functional foods include any natural product that presents health-promoting effects, thereby reducing the risk of chronic diseases. Cerrado fruits are considered a source of bioactive substances, mainly phenolic compounds, making them important functional foods. Despite this, the losses of natural vegetation in the Cerrado are progressive. Hence, the knowledge propagation about the importance of the species found in Cerrado could contribute to the preservation of this biome. This review provides information about Cerrado fruits and highlights the structures and pharmacologic potential of functional compounds found in these fruits. Compounds detected in Caryocar brasiliense Camb. (pequi, Dipteryx alata Vog. (baru, Eugenia dysenterica DC. (cagaita, Eugenia uniflora L. (pitanga, Genipa americana L. (jenipapo, Hancornia speciosa Gomes (mangaba, Mauritia flexuosa L.f. (buriti, Myrciaria cauliflora (DC Berg (jabuticaba, Psidium guajava L. (goiaba, Psidium spp. (araçá, Solanum lycocarpum St. Hill (lobeira, Spondias mombin L. (cajá, Annona crassiflora Mart. (araticum, among others are reported here.

  15. Wetspun poly-L-(lactic acid)-borosilicate bioactive glass scaffolds for guided bone regeneration

    Energy Technology Data Exchange (ETDEWEB)

    Fernandes, João S., E-mail: joao.fernandes@dep.uminho.pt [3B' s Research Group - Biomaterials, Biodegradables and Biomimetics, University of Minho, Headquarters of the European Institute of Excellence on Tissue Engineering and Regenerative Medicine, AvePark-Parque de Ciência e Tecnologia, Zona Industrial da Gandra, 4805-017 Barco GMR (Portugal); ICVS/3B' s - PT Government Associate Laboratory, Braga/Guimarães (Portugal); Reis, Rui L. [3B' s Research Group - Biomaterials, Biodegradables and Biomimetics, University of Minho, Headquarters of the European Institute of Excellence on Tissue Engineering and Regenerative Medicine, AvePark-Parque de Ciência e Tecnologia, Zona Industrial da Gandra, 4805-017 Barco GMR (Portugal); ICVS/3B' s - PT Government Associate Laboratory, Braga/Guimarães (Portugal); Pires, Ricardo A., E-mail: rpires@dep.uminho.pt [3B' s Research Group - Biomaterials, Biodegradables and Biomimetics, University of Minho, Headquarters of the European Institute of Excellence on Tissue Engineering and Regenerative Medicine, AvePark-Parque de Ciência e Tecnologia, Zona Industrial da Gandra, 4805-017 Barco GMR (Portugal); ICVS/3B' s - PT Government Associate Laboratory, Braga/Guimarães (Portugal)

    2017-02-01

    We developed a porous poly-L-lactic acid (PLLA) scaffold compounded with borosilicate bioactive glasses (BBGs) endowing it with bioactive properties. Porous PLLA-BBG fibre mesh scaffolds were successfully prepared by the combination of wet spinning and fibre bonding techniques. Micro-computed tomography (μCT) confirmed that the PLLA-BBG scaffolds containing ≈ 25% of BBGs (w/w) exhibited randomly interconnected porous (58 to 62% of interconnectivity and 53 to 67% of porosity) with mean pore diameters higher that 100 μm. Bioactivity and degradation studies were performed by immersing the scaffolds in simulated body fluid (SBF) and ultrapure water, respectively. The PLLA-BBG scaffolds presented a faster degradation rate with a constant release of inorganic species, which are capable to produce calcium phosphate structures at the surface of the material after 7 days of immersion in SBF (Ca/P ratio of ~ 1.7). Cellular in vitro studies with human osteosarcoma cell line (Saos-2) and human adipose-derived stem cells (hASCs) showed that PLLA-BBGs are not cytotoxic to cells, while demonstrating their capacity to promote cell adhesion and proliferation. Overall, we showed that the proposed scaffolds present a tailored kinetics on the release of inorganic species and controlled biological response under conditions that mimic the bone physiological environment. - Highlights: • We prepared borosilicate glasses and their PLLA composites in the form of fibres. • These glasses imparted bioactivity and controlled degradability to the fibres. • The prepared fibres did not elicit cytotoxicity. • hASCs attached and proliferated in the surface and inner sections of the scaffolds. • The composites present appropriate properties to be used in bone tissue engineering.

  16. Atmospheric Precipitations, Hailstone and Rainwater, as a Novel Source of Streptomyces Producing Bioactive Natural Products

    Science.gov (United States)

    Sarmiento-Vizcaíno, Aida; Espadas, Julia; Martín, Jesús; Braña, Alfredo F.; Reyes, Fernando; García, Luis A.; Blanco, Gloria

    2018-01-01

    A cultivation-dependent approach revealed that highly diverse populations of Streptomyces were present in atmospheric precipitations from a hailstorm event sampled in February 2016 in the Cantabrian Sea coast, North of Spain. A total of 29 bioactive Streptomyces strains isolated from small samples of hailstone and rainwater, collected from this hailstorm event, were studied here. Taxonomic identification by 16S rRNA sequencing revealed more than 20 different Streptomyces species, with their closest homologs displaying mainly oceanic but also terrestrial origins. Backward trajectory analysis revealed that the air-mass sources of the hailstorm event, with North Western winds, were originated in the Arctic Ocean (West Greenland and North Iceland) and Canada (Labrador), depending on the altitude. After traveling across the North Atlantic Ocean during 4 days the air mass reached Europe and precipitated as hailstone and rain water at the sampling place in Spain. The finding of Streptomyces species able to survive and disperse through the atmosphere increases our knowledge of the biogeography of genus Streptomyces on Earth, and reinforces our previous dispersion model, suggesting a generalized feature for the genus which could have been essential in his evolution. This unique atmospheric-derived Streptomyces collection was screened for production of bioactive secondary metabolites. Analyses of isolates ethyl acetate extracts by LC-UV-MS and further database comparison revealed an extraordinary diversity of bioactive natural products. One hundred molecules were identified, mostly displaying contrasted antibiotic and antitumor/cytotoxic activities, but also antiparasitic, antiviral, anti-inflammatory, neuroprotector, and insecticide properties. More interestingly, 38 molecules not identified in natural products databases might represent new natural products. Our results revealed for the first time an extraordinary diversity of Streptomyces species in the atmosphere able to

  17. Wetspun poly-L-(lactic acid)-borosilicate bioactive glass scaffolds for guided bone regeneration

    International Nuclear Information System (INIS)

    Fernandes, João S.; Reis, Rui L.; Pires, Ricardo A.

    2017-01-01

    We developed a porous poly-L-lactic acid (PLLA) scaffold compounded with borosilicate bioactive glasses (BBGs) endowing it with bioactive properties. Porous PLLA-BBG fibre mesh scaffolds were successfully prepared by the combination of wet spinning and fibre bonding techniques. Micro-computed tomography (μCT) confirmed that the PLLA-BBG scaffolds containing ≈ 25% of BBGs (w/w) exhibited randomly interconnected porous (58 to 62% of interconnectivity and 53 to 67% of porosity) with mean pore diameters higher that 100 μm. Bioactivity and degradation studies were performed by immersing the scaffolds in simulated body fluid (SBF) and ultrapure water, respectively. The PLLA-BBG scaffolds presented a faster degradation rate with a constant release of inorganic species, which are capable to produce calcium phosphate structures at the surface of the material after 7 days of immersion in SBF (Ca/P ratio of ~ 1.7). Cellular in vitro studies with human osteosarcoma cell line (Saos-2) and human adipose-derived stem cells (hASCs) showed that PLLA-BBGs are not cytotoxic to cells, while demonstrating their capacity to promote cell adhesion and proliferation. Overall, we showed that the proposed scaffolds present a tailored kinetics on the release of inorganic species and controlled biological response under conditions that mimic the bone physiological environment. - Highlights: • We prepared borosilicate glasses and their PLLA composites in the form of fibres. • These glasses imparted bioactivity and controlled degradability to the fibres. • The prepared fibres did not elicit cytotoxicity. • hASCs attached and proliferated in the surface and inner sections of the scaffolds. • The composites present appropriate properties to be used in bone tissue engineering.

  18. Rare actinomycetes Nocardia caishijiensis and Pseudonocardia carboxydivorans as endophytes, their bioactivity and metabolites evaluation.

    Science.gov (United States)

    Tanvir, Rabia; Sajid, Imran; Hasnain, Shahida; Kulik, Andreas; Grond, Stephanie

    2016-04-01

    Two strains identified as Nocardia caishijiensis (SORS 64b) and Pseudonocardia carboxydivorans (AGLS 2) were isolated as endophytes from Sonchus oleraceus and Ageratum conyzoides respectively. The analysis of their extracts revealed them to be strongly bioactive. The N. caishijiensis extract gave an LC50 of 570 μg/ml(-1) in the brine shrimp cytotoxicity assay and an EC50 of 0.552 μg/ml(-1) in the DPPH antioxidant assay. Antimicrobial activity was observed against Methicillin resistant Staphlococcus aureus (MRSA) and Escherichia coli ATCC 25922 (14 mm), Klebsiella pneumoniae ATCC 706003 (13 mm), S. aureus ATCC 25923 (11 mm) and Candida tropicalis (20 mm). For the extract of P. carboxydivorans the EC50 was 0.670 μg/ml(-1) and it was observed to be more bioactive against Bacillus subtilis DSM 10 ATCC 6051 (21 mm), C. tropicalis (20 mm), S. aureus ATCC 25923 (17 mm), MRSA (17 mm), E. coli K12 (W1130) (16 mm) and Chlorella vulgaris (10 mm). The genotoxicity testing revealed a 20 mm zone of inhibition against the polA mutant strain E. coli K-12 AB 3027 suggesting damage to the DNA and polA genes. The TLC and bioautography screening revealed a diversity of active bands of medium polar and nonpolar compounds. Metabolite analysis by HPLC-DAD via UV/vis spectral screening suggested the possibility of stenothricin and bagremycin A in the mycelium extract of N. caishijiensis respectively. In the broth and mycelium extract of P. carboxydivorans borrelidin was suggested along with α-pyrone. The HPLC-MS revealed bioactive long chained amide derivatives such as 7-Octadecenamide, 9, 12 octadecandienamide. This study reports the rare actinomycetes N. caishijiensis and P. carboxydivorans as endophytes and evaluates their bioactive metabolites. Copyright © 2016 Elsevier GmbH. All rights reserved.

  19. Development of Bioactive Ceramic Coating on Titanium Alloy substrate for Biomedical Application Using Dip Coating Method

    Science.gov (United States)

    Asmawi, R.; Ibrahim, M. H. I.; Amin, A. M.; Mustafa, N.; Noranai, Z.

    2017-08-01

    Bioactive apatite, such as hydroxyapatite ceramic (HA), [Ca10(PO4)6(OH)2] has been extensively investigated for biomedical applications due to its excellent biocompatibility and tissue bioactivity properties. Its bioactivity provides direct bonding to the bone tissue. Because of its similarity in chemical composition to the inorganic matrix of bone, HA is widely used as implant materials for bone. Unfortunately, because of its poor mechanical properties,. this bioactive material is not suitable for load bearing applications. In this study, by the assistance of dip-coating technique, HA coatings were deposited on titanium alloy substrates by employing hydrothermal derived HA powder. The produced coatings then were oven-dried at 130°C for 1 hour and calcined at various temperature over the range of 200-800°C for 1 hour. XRD measurement showed that HA was the only phase present in the coatings. However coatings calcined at 800°C comprised a mixture of HA and tri-calcium phosphate (TCP). FTIR measurement showed the existence of hydroxyl, phosphate, and carbonate bands. PO4 - band became sharper and narrower with the increased of calcination temperature. FESEM observation showed that the coating is polycrystalline with individual particles of nano to submicron size and has an average particle size of 35 nm. The thickness of the coating are direcly propotional with the viscosity of coating slurry. It was shown that the more viscous coating slurry would produce a thicker ceramic coating. Mechanical properties of the coating were measured in term of adhesion strength using a Micro Materials Nano Test microscratch testing machine. The result revealed that the coating had a good adhesion to the titanium alloy substrate.

  20. Bioactive Peptides in Cereals and Legumes: Agronomical, Biochemical and Clinical Aspects

    Directory of Open Access Journals (Sweden)

    Marco Malaguti

    2014-11-01

    Full Text Available Cereals and legumes are key components of a healthy and balanced diet. Accordingly, many national nutritional guidelines emphasize their health promoting properties by placing them at the base of nutritional food pyramids. This concept is further validated by the observed correlation between a lower risk and occurrence of chronic diseases and the adherence to dietary patterns, like the Mediterranean diet, in which cereal grains, legumes and derived products represent a staple food. In the search for a dietary approach to control/prevent chronic degenerative diseases, protein derived bioactive peptides may represent one such source of health-enhancing components. These peptides may already be present in foods as natural components or may derive from hydrolysis by chemical or enzymatic treatments (digestion, hydrolysis or fermentation. Many reports are present in the literature regarding the bioactivity of peptides in vitro and a wide range of activities has been described, including antimicrobial properties, blood pressure-lowering (ACE inhibitory effects, cholesterol-lowering ability, antithrombotic and antioxidant activities, enhancement of mineral absorption/bioavailability, cyto- or immunomodulatory effects, and opioid-like activities. However it is difficult to translate these observed effects to human. In fact, the active peptide may be degraded during digestion, or may not be absorbed or reach the target tissues at a concentration necessary to exert its function. This review will focus on bioactive peptides identified in cereals and legumes, from an agronomical and biochemical point of view, including considerations about requirements for the design of appropriate clinical trials necessary for the assessment of their nutraceutical effect in vivo.

  1. House dust bioactivities predict skin prick test reactivity for children with high risk of allergy.

    Science.gov (United States)

    Kim, Haejin; Tse, Kevin; Levin, Linda; Bernstein, David; Reponen, Tiina; LeMasters, Grace; Lummus, Zana; Horner, Anthony A

    2012-06-01

    Although evidence suggests that ambient exposures to endotoxin and other immunostimulants during early life influence allergic risk, efforts to understand this host-environment relationship have been hampered by a paucity of relevant assays. These investigations determined whether parameters of house dust extract (HDE) bioactivity were predictive of allergen skin prick test (SPT) reactivity for infants at high risk of allergy participating in the Cincinnati Childhood Allergy and Air Pollution Study (CCAAPS). We conducted a nested case-control study, selecting 99 CCAAPS children who had positive SPT results to at least 1 aeroallergen at age 3 years and 101 subjects with negative SPT results. HDEs were prepared from dust samples collected from the subjects' homes at age 1 year. Murine splenocytes and bone marrow-derived dendritic cells were incubated with HDEs, and supernatant cytokine concentrations were determined by means of ELISA. Alternatively, bone marrow-derived dendritic cells were preincubated with HDEs, and then LPS-induced IL-6 responses were assessed. HDE endotoxin levels were determined by using the limulus amebocyte lysate assay. HDEs derived from the homes of children with positive (cases) and negative (control subjects) SPT results had similar bioactivities. However, when cases were considered in isolation, HDEs with higher levels of bioactivity were significantly associated with children who had lower numbers of positive SPT results. Analogous statistical analyses did not identify any association between HDE endotoxin levels and the aeroallergen sensitization profiles of children included in this study. HDE immunostimulatory activities predicted the aeroallergen sensitization status of CCAAPS subjects better than HDE endotoxin levels. These results provide the first published evidence that HDE bioassays have clinical relevance in predicting atopic risk. Copyright © 2012 American Academy of Allergy, Asthma & Immunology. Published by Mosby, Inc. All

  2. Characterization,Mechanical, and In Vitro Bioactivity Properties of Hydroxyapatite/Bioactive Glass Composite

    Directory of Open Access Journals (Sweden)

    Israa Kahatan Sabree

    2016-12-01

    Full Text Available Bioactive ceramic materials can help bone reparation and regeneration by offering support to bone growth. Biological hydroxyapatite powder was prepared by burning animal bone followed by studying the mechanical properties of hydroxyapatite (HA/ (20wt.%, and 40wt.% of binary bioactive glass (70% SiO2- 30% CaO in order to evaluate the influence of composition on the compressive strength and hardness. HA-composite material exhibited increasing density, microhardness, and compressive strength with increasing amount of glass addition. X-ray diffraction after sintering at 1200°C showed no alter of HA to secondary phases while the hydroxyapatite/ bioactive glass composites contained a HA phase and different amounts of wollastonite phase, depending on the amount of bioglass added. In vitro tests, the samples were soaked in simulated body fluid (SBF for ten days in order to evaluate the change in compression strength, weight loss, and pH. The HA composite reinforced with 40 wt % bioglass showed highest compression strength, and lowest weight loss

  3. Antioxidant capacity and bioactive compounds of four Brazilian native fruits

    Directory of Open Access Journals (Sweden)

    Cristiane C. Denardin

    2015-09-01

    Full Text Available The purpose of this study was to evaluate the bioactive compounds and antioxidant activity of extracts from araçá (Psidium cattleianum, butiá (Butia eriospatha, and pitanga (Eugenia uniflora fruits with different flesh colors (i.e., purple, red, and orange, and blackberries (Rubus sp.; cv. Xavante and Cherokee collected in the southern region of Brazil. The content of ascorbic acid, total carotenoids, and phenolics were determined. The profile of the phenolic compounds was assessed by high-performance liquid chromatography combined with diode array detection (HPLC-DAD. The antioxidant activity was determined using the ferric-reducing antioxidant power (FRAP assay, 2,2-diphenyl-2-picrylhydrazyl hydrate (DPPH assay, total reactive antioxidant potential (TRAP assay, and total antioxidant reactivity (TAR assay. The Xavante blackberry and purple-fleshed pitanga showed the highest total phenolic content [816.50 mg gallic acid equivalents (GAE/100g and 799.80 mg GAE/100g, respectively]. The araçá and red-fleshed pitanga showed the highest carotenoid content (6.27 ug β-carotene/g and 5.86 ug β-carotene/g, respectively. The fruits contained several phenolic compounds such as quercetin derivatives, quercitrin, isoquercitrin, and cyanidin derivatives, which may contribute differentially to the antioxidant capacity. The highest scavenging activity in the DPPH assay was found for purple-fleshed pitanga (IC50 36.78 mg/L, blackberries [IC50 44.70 (Xavante and IC50 78.25 mg/L (Cherokee], and araçá (IC50 48.05 mg/L, which also showed the highest FRAP, followed by orange- and red-fleshed pitanga. Our results revealed that some fruits grown in southern Brazil such as purple-fleshed pitanga, blackberries, and araçá are rich sources of phenolic compounds and have great antioxidant activity.

  4. Bactericidal strontium-releasing injectable bone cements based on bioactive glasses

    OpenAIRE

    Brauer, Delia S.; Karpukhina, Natalia; Kedia, Gopal; Bhat, Aditya; Law, Robert V.; Radecka, Izabela; Hill, Robert G.

    2013-01-01

    Strontium-releasing injectable bone cements may have the potential to prevent implant-related infections through the bactericidal action of strontium, while enhancing bone formation in patients suffering from osteoporosis. A melt-derived bioactive glass (BG) series (SiO2–CaO–CaF2–MgO) with 0–50% of calcium substituted with strontium on a molar base were produced. By mixing glass powder, poly(acrylic acid) and water, cements were obtained which can be delivered by injection and set in situ, gi...

  5. One-pot synthesis of bioactive cyclopentenones from α-linolenic acid and docosahexaenoic acid.

    Science.gov (United States)

    Maynard, Daniel; Müller, Sara Mareike; Hahmeier, Monika; Löwe, Jana; Feussner, Ivo; Gröger, Harald; Viehhauser, Andrea; Dietz, Karl-Josef

    2018-04-01

    Oxidation products of the poly-unsaturated fatty acids (PUFAs) arachidonic acid, α-linolenic acid and docosahexaenoic acid are bioactive in plants and animals as shown for the cyclopentenones prostaglandin 15d-PGJ 2 and PGA 2 , cis-(+)-12-oxophytodienoic acid (12-OPDA), and 14-A-4 neuroprostane. In this study an inexpensive and simple enzymatic multi-step one-pot synthesis is presented for 12-OPDA, which is derived from α-linolenic acid, and the analogous docosahexaenoic acid (DHA)-derived cyclopentenone [(4Z,7Z,10Z)-12-[[-(1S,5S)-4-oxo-5-(2Z)-pent-2-en-1yl]-cyclopent-2-en-1yl] dodeca-4,7,10-trienoic acid, OCPD]. The three enzymes utilized in this multi-step cascade were crude soybean lipoxygenase or a recombinant lipoxygenase, allene oxide synthase and allene oxide cyclase from Arabidopsis thaliana. The DHA-derived 12-OPDA analog OCPD is predicted to have medicinal potential and signaling properties in planta. With OCPD in hand, it is shown that this compound interacts with chloroplast cyclophilin 20-3 and can be metabolized by 12-oxophytodienoic acid reductase (OPR3) which is an enzyme relevant for substrate bioactivity modulation in planta. Copyright © 2017 Elsevier Ltd. All rights reserved.

  6. Bioactivity of gel-glass powders in the CaO-SiO2 system: a comparison with ternary (CaO-P2O5-SiO2) and quaternary glasses (SiO2-CaO-P2O5-Na2O).

    Science.gov (United States)

    Saravanapavan, Priya; Jones, Julian R; Pryce, Russell S; Hench, Larry L

    2003-07-01

    Bioactive glasses react chemically with body fluids in a manner that is compatible with the repair processes of the tissues. This results in the formation of an interfacial bond between the glasses and living tissue. Bioactive glasses also stimulate bone-cell proliferation. This behavior is dependent on the chemical composition as well as the surface texture of the glasses. It has been recently reported that gel-derived monolith specimens in the binary SiO2 - CaO are bioactive over a similar molar range of SiO2 content as the previously studied ternary CaO-P2O5-SiO2 system. In this report, the preparation and bioactivity of the binary gel-glass powder with 70 mol % SiO2 is discussed and its bioactivity is compared with the melt-derived 45S5 (quaternary) Bioglass and sol-gel-derived 58S (ternary) bioactive gel-glass compositions. Dissolution kinetic parameters K(1) and K(2) were also computed based on the silicon release for all glass powders. It was shown that the simple two-component SiO2-CaO gel-glass powder is bioactive with comparable dissolution rates as the clinically used melt-derived 45S5 Bioglass powder and extensively studied sol-gel-derived 58S gel-glass powder. Copyright 2003 Wiley Periodicals, Inc.

  7. In vitro bioactivity and antimicrobial tuning of bioactive glass nanoparticles added with neem (Azadirachta indica) leaf powder.

    Science.gov (United States)

    Prabhu, M; Ruby Priscilla, S; Kavitha, K; Manivasakan, P; Rajendran, V; Kulandaivelu, P

    2014-01-01

    Silica and phosphate based bioactive glass nanoparticles (58SiO2-33CaO-9P2O5) with doping of neem (Azadirachta indica) leaf powder and silver nanoparticles were prepared and characterised. Bioactive glass nanoparticles were produced using sol-gel technique. In vitro bioactivity of the prepared samples was investigated using simulated body fluid. X-ray diffraction (XRD) pattern of prepared glass particles reveals amorphous phase and spherical morphology with a particle size of less than 50 nm. When compared to neem doped glass, better bioactivity was attained in silver doped glass through formation of hydroxyapatite layer on the surface, which was confirmed through XRD, Fourier transform infrared (FTIR), and scanning electron microscopy (SEM) analysis. However, neem leaf powder doped bioactive glass nanoparticles show good antimicrobial activity against Staphylococcus aureus and Escherichia coli and less bioactivity compared with silver doped glass particles. In addition, the biocompatibility of the prepared nanocomposites reveals better results for neem doped and silver doped glasses at lower concentration. Therefore, neem doped bioactive glass may act as a potent antimicrobial agent for preventing microbial infection in tissue engineering applications.

  8. In Vitro Bioactivity and Antimicrobial Tuning of Bioactive Glass Nanoparticles Added with Neem (Azadirachta indica) Leaf Powder

    Science.gov (United States)

    Prabhu, M.; Ruby Priscilla, S.; Kavitha, K.; Manivasakan, P.; Rajendran, V.; Kulandaivelu, P.

    2014-01-01

    Silica and phosphate based bioactive glass nanoparticles (58SiO2-33CaO-9P2O5) with doping of neem (Azadirachta indica) leaf powder and silver nanoparticles were prepared and characterised. Bioactive glass nanoparticles were produced using sol-gel technique. In vitro bioactivity of the prepared samples was investigated using simulated body fluid. X-ray diffraction (XRD) pattern of prepared glass particles reveals amorphous phase and spherical morphology with a particle size of less than 50 nm. When compared to neem doped glass, better bioactivity was attained in silver doped glass through formation of hydroxyapatite layer on the surface, which was confirmed through XRD, Fourier transform infrared (FTIR), and scanning electron microscopy (SEM) analysis. However, neem leaf powder doped bioactive glass nanoparticles show good antimicrobial activity against Staphylococcus aureus and Escherichia coli and less bioactivity compared with silver doped glass particles. In addition, the biocompatibility of the prepared nanocomposites reveals better results for neem doped and silver doped glasses at lower concentration. Therefore, neem doped bioactive glass may act as a potent antimicrobial agent for preventing microbial infection in tissue engineering applications. PMID:25276834

  9. Thermoluminescence as a probe in bioactivity studies; the case of 58S sol-gel bioactive glass

    International Nuclear Information System (INIS)

    Polymeris, George S; Tsirliganis, Nestor C; Goudouri, Ourania Menti; Paraskevopoulos, Konstantinos M; Kontonasaki, Eleana; Kitis, George

    2011-01-01

    The formation of a carbonated hydroxyapatite (HCAp) layer on the surface of bioactive materials is the main reaction that takes place upon their immersion in physiological fluids. To date, all techniques used for the identification of this HCAp formation are rather time consuming and not well suited to detailed and rapid monitoring of changes in the bioactivity response of the material. The aim of this work is to explore the possibility of using thermoluminescence (TL) for the discrimination between different bioactive responses in the case of the 58S bioactive glass. Results provided strong indications that the 110 deg. C TL peak of quartz can be used effectively in the study of the bioactive behaviour of 58S bioactive glass, since it is unambiguously present in all samples and does not require deconvolution analysis. Furthermore, the intensity of the 110 deg. C TL peak is proven to be very sensitive to the different bioactive responses, identifying the loss of silica which takes place at the first stages of the sequence. The discontinuities of the 110 deg. C TL peak intensity plot versus immersion time at 8 and 1440 min provide experimental indications regarding the timescale for both the beginning of amorphous CaP formation as well as the end of crystalline hydroxyl-apatite formation respectively, while the spike in the sensitization of the 110 deg. C TL peak, which was observed for immersion times ranging between 20 and 40 min, could be an experimental feature indicating the beginning of the crystalline HCAp formation.

  10. Stereochemical determination and bioactivity assessment of {(S)}-(+)-curcuphenol dimers isolated from the marine sponge Didiscus aceratus and synthesized through laccase biocatalysis

    DEFF Research Database (Denmark)

    Lassen, Peter Rygaard

    2005-01-01

    Electrospray ionization mass spectrometry-guided isolation of extracts from Didiscus aceratus led to the discovery of several new derivatives of the bioactive bisabolene-type sponge metabolite (S)-(+)-curcuphenol (1). The compounds obtained by this method included a mixture of known (2) and new (3...

  11. Bioactive proteins against pathogenic and spoilage bacteria

    Directory of Open Access Journals (Sweden)

    Mahmoud Z. Sitohy

    2014-10-01

    Full Text Available Background: It is likely that both human nutrition and the nutrition of livestock are benefited by the presence of bioactive proteins within their respective diet regimes. Bioactive proteins have been defined as specific protein fragments that positively impact bodily functions or conditions and may, ultimately, influence overall human health. The ingestion of bioactive proteins may have an effect on the major body systems—namely, the cardiovascular, digestive, immune and nervous systems. According to their functional properties, bioactive proteins may be classified as antimicrobial, antithrombotic, antihypertensive, opioid, immune-modulatory, mineral binding and anti-oxidative. There are many examples of biologically active food proteins and active peptides that can be obtained from various food protein sources. They have a physiological significance beyond the pure nutritional requirements; in other wordsthey have the acquisition of nitrogen for normal growth and maintenance. Objective: This study aims to specify and characterize the extent and mode of action of bioactive proteins in their native form, (glycinin, glycinin basic sub-unit and β-conglycinin against specific main pathogens (Listeria monocytogenes, Escherichia coli O157:H7 and Salmonella enterica serovar Enteritidis. We will be using standard media while identifying the main constituents responsible for this action. Methods: Glycinin, basic sub-unit and β-conglycinin were isolated from soybean protein and tested for their antimicrobial action against pathogenic and spoilage bacteria, They were thencompared to the properties of penicillin. Methylated soybean protein and also methylated chickpea protein (MSP and MCP, with isoelectric points around pI 8, were prepared by esterifying. 83 % of their free carboxyl groups and their interactions with Gram positive and Gram negative bacteria were examined. Results: The three divisions of cationic proteins exhibited antibacterial

  12. Metabolite analysis of endophytic fungi from cultivars of Zingiber officinale Rosc. identifies myriad of bioactive compounds including tyrosol.

    Science.gov (United States)

    Anisha, C; Radhakrishnan, E K

    2017-06-01

    Endophytic fungi associated with rhizomes of four cultivars of Zingiber officinale were identified by molecular and morphological methods and evaluated for their activity against soft rot pathogen Pythium myriotylum and clinical pathogens. The volatile bioactive metabolites produced by these isolates were identified by GC-MS analysis of the fungal crude extracts. Understanding of the metabolites produced by endophytes is also important in the context of raw consumption of ginger as medicine and spice. A total of fifteen isolates were identified from the four varieties studied. The various genera identified were Acremonium sp., Gliocladiopsis sp., Fusarium sp., Colletotrichum sp., Aspergillus sp., Phlebia sp., Earliella sp., and Pseudolagarobasidium sp. The endophytic community was unique to each variety, which could be due to the varying host genotype. Fungi from phylum Basidiomycota were identified for the first time from ginger. Seven isolates showed activity against Pythium, while only two showed antibacterial activity. The bioactive metabolites identified in the fungal crude extracts include tyrosol, benzene acetic acid, ergone, dehydromevalonic lactone, N-aminopyrrolidine, and many bioactive fatty acids and their derivatives which included linoleic acid, oleic acid, myristic acid, n-hexadecanoic acid, palmitic acid methyl ester, and methyl linoleate. The presence of these varying bioactive endophytic fungi may be one of the reasons for the differences in the performance of the different ginger varieties.

  13. Towards generation of bioactive peptides from meat industry waste proteins: Generation of peptides using commercial microbial proteases.

    Science.gov (United States)

    Ryder, Kate; Bekhit, Alaa El-Din; McConnell, Michelle; Carne, Alan

    2016-10-01

    Five commercially available food-grade microbial protease preparations were evaluated for their ability to hydrolyse meat myofibrillar and connective tissue protein extracts to produce bioactive peptides. A bacterial-derived protease (HT) extensively hydrolysed both meat protein extracts, producing peptide hydrolysates with significant in vitro antioxidant and ACE inhibitor activities. The hydrolysates retained bioactivity after simulated gastrointestinal hydrolysis challenge. Gel permeation chromatography sub-fractionation of the crude protein hydrolysates showed that the smaller peptide fractions exhibited the highest antioxidant and ACE inhibitor activities. OFFGEL electrophoresis of the small peptides of both hydrolysates showed that low isoelectric point peptides had antioxidant activity; however, no consistent relationship was observed between isoelectric point and ACE inhibition. Cell-based assays indicated that the hydrolysates present no significant cytotoxicity towards Vero cells. The results indicate that HT protease hydrolysis of meat myofibrillar and connective tissue protein extracts produces bioactive peptides that are non-cytotoxic, should be stable in the gastrointestinal tract and may contain novel bioactive peptide sequences. Copyright © 2016 Elsevier Ltd. All rights reserved.

  14. History and trends of bioactive glass-ceramics.

    Science.gov (United States)

    Montazerian, Maziar; Dutra Zanotto, Edgar

    2016-05-01

    The interest around bioactive glass-ceramics (GCs) has grown significantly over the last two decades due to their appropriate biochemical and mechanical properties. The intense research effort in this field has led to some new commercial products for biomedical applications. This review article begins with the basic concepts of GC processing and development via controlled heat treatments of monolithic pieces or sinter-crystallization of powdered glasses. We then go on to describe the processing, properties, and applications of some commercial bioactive GCs and discuss selected valuable reported researches on several promising types of bioactive GCs. The article finishes with a section on open relevant research directions for bioactive GC development. © 2016 Wiley Periodicals, Inc.

  15. Fruit and cereal bioactives: sources, chemistry, and applications

    National Research Council Canada - National Science Library

    Tokusoglu, Ozlem; Hall, Clifford, III

    2011-01-01

    "Presenting up-to-date data in an easy-to-use format, this comprehensive overview of the chemistry of bioactive components of fruits and cereals addresses the role of these compounds in determining...

  16. Bioactive foods in promoting health: probiotics and prebiotics

    National Research Council Canada - National Science Library

    Watson, Ronald R; Preedy, Victor R

    2010-01-01

    "Bioactive Foods in Health Promotion: Probiotics and Prebiotics brings together experts working on the different aspects of supplementation, foods, and bacterial preparations, in health promotion and disease prevention, to provide...

  17. Abrasive wear behaviour of bio-active glass ceramics containing ...

    Indian Academy of Sciences (India)

    Unknown

    Technical Education Faculty, Mersin University, 33480 Tarsus, Turkey. MS received 18 October 2005; revised 22 March 2006. Abstract. In this study, abrasive ... process were used to produce bio-active ceramics. Fracture toughness of studied ...

  18. Current Strategies to Improve the Bioactivity of PEEK

    Science.gov (United States)

    Ma, Rui; Tang, Tingting

    2014-01-01

    The synthetic thermoplastic polymer polyetheretherketone (PEEK) is becoming a popular component of clinical orthopedic and spinal applications, but its practical use suffers from several limitations. Although PEEK is biocompatible, chemically stable, radiolucent and has an elastic modulus similar to that of normal human bone, it is biologically inert, preventing good integration with adjacent bone tissues upon implantation. Recent efforts have focused on increasing the bioactivity of PEEK to improve the bone-implant interface. Two main strategies have been used to overcome the inert character of PEEK. One approach is surface modification to activate PEEK through surface treatment alone or in combination with a surface coating. Another strategy is to prepare bioactive PEEK composites by impregnating bioactive materials into PEEK substrate. Researchers believe that modified bioactive PEEK will have a wide range of orthopedic applications. PMID:24686515

  19. Bioactive compounds in seaweed; functional food applications and legislation

    DEFF Research Database (Denmark)

    Holdt, Susan Løvstad; Kraan, Stefan

    2011-01-01

    Seaweed is more than the wrap that keeps rice together in sushi. Seaweed biomass is already used for a wide range of other products in food, including stabilising agents. Biorefineries with seaweed as feedstock are attracting worldwide interest and include low-volume, high value-added products...... and vice versa. Scientific research on bioactive compounds in seaweed usually takes place on just a few species and compounds. This paper reviews worldwide research on bioactive compounds, mainly of nine genera or species of seaweed, which are also available in European temperate Atlantic waters, i...... described in this review. This applies either to the choice of high value-added bioactive products to be exploited in an available species or to the choice of seaweed species when a bioactive compound is desired. Data are presented in tables with species, effect and test organism (if present) with examples...

  20. Modeling of Viscosity and Thermal Expansion of Bioactive Glasses

    OpenAIRE

    Farid, Saad B. H.

    2012-01-01

    The behaviors of viscosity and thermal expansion for different compositions of bioactive glasses have been studied. The effect of phosphorous pentoxide as a second glass former in addition to silica was investigated. Consequently, the nonlinear behaviors of viscosity and thermal expansion with respect to the oxide composition have been modeled. The modeling uses published data on bioactive glass compositions with viscosity and thermal expansion. -regression optimization technique has been uti...

  1. Bioactive endodontic materials for everyday use: a review.

    Science.gov (United States)

    Walsh, Ryan M; He, Jianing; Schweitzer, Jordan; Opperman, Lynne A; Woodmansey, Karl F

    2018-01-01

    Bioceramic materials are at the forefront of modern dentistry. Bioactive bioceramic endodontic materials promote pulpal and periapical tissue healing and are easy to use. Dentists can choose among many endodontic materials, depending on their needs. This article highlights the major differences among commercially available bioactive tricalcium silicate bioceramics, commonly known as mineral trioxide aggregate materials, to enable dentists to make appropriate decisions in the selection of these materials.

  2. Whey Based Bioactive Peptides Used in Animal Products

    Directory of Open Access Journals (Sweden)

    Ayse Demet Karaman

    2016-10-01

    Full Text Available Bioactive peptides come out as a result of the hydrolysis of milk proteins and contain nutritional, functional and biological activities. Nowadays, the utilization of whey proteins to provide various features in the animal products such as meat and milk products and animal production has been increasing. In this compilation, after being introduced some general information about their common characteristics, bioactive peptides will be mentioned about their particularly recent usage in animal products.

  3. Cell Based Meniscal Repair Using an Aligned Bioactive Nanofibrous Sheath

    Science.gov (United States)

    2017-07-01

    to subsequently guide tissue regeneration , for example, by seeded tissue progenitor cells . To achieve this objective, the first step is to develop...AWARD NUMBER: W81XWH-15-1-0104 TITLE: Cell -Based Meniscal Repair Using an Aligned Bioactive Nanofibrous Sheath PRINCIPAL INVESTIGATOR...SUBTITLE 5a. CONTRACT NUMBER Cell -Based Meniscal Repair Using an Aligned Bioactive Nanofibrous Sheath 5b. GRANT NUMBER W81XWH-15-1-0104 5c. PROGRAM

  4. Mesoporous Bioactive Glass Functionalized 3D Ti-6Al-4V Scaffolds with Improved Surface Bioactivity.

    Science.gov (United States)

    Ye, Xiaotong; Leeflang, Sander; Wu, Chengtie; Chang, Jiang; Zhou, Jie; Huan, Zhiguang

    2017-10-27

    Porous Ti-6Al-4V scaffolds fabricated by means of selective laser melting (SLM), having controllable geometrical features and preferable mechanical properties, have been developed as a class of biomaterials that hold promising potential for bone repair. However, the inherent bio-inertness of the Ti-6Al-4V alloy as the matrix of the scaffolds results in a lack in the ability to stimulate bone ingrowth and regeneration. The aim of the present study was to develop a bioactive coating on the struts of SLM Ti-6Al-4V scaffolds in order to add the desired surface osteogenesis ability. Mesoporous bioactive glasses (MBGs) coating was applied on the strut surfaces of the SLM Ti-6Al-4V scaffolds through spin coating, followed by a heat treatment. It was found that the coating could maintain the characteristic mesoporous structure and chemical composition of MBG, and establish good interfacial adhesion to the Ti-6Al-4V substrate. The compressive strength and pore interconnectivity of the scaffolds were not affected by the coating. Moreover, the results obtained from in vitro cell culture experiments demonstrated that the attachment, proliferation, and differentiation of human bone marrow stromal cells (hBMSCs) on the MBG-coated Ti-6Al-4V scaffolds were improved as compared with those on the conventional bioactive glass (BG)-coated Ti-6Al-4V scaffolds and bare-metal Ti-6Al-4V scaffolds. Our results demonstrated that the MBG coating by using the spinning coating method could be an effective approach to achieving enhanced surface biofunctionalization for SLM Ti-6Al-4V scaffolds.

  5. Mesoporous Bioactive Glass Functionalized 3D Ti-6Al-4V Scaffolds with Improved Surface Bioactivity

    Directory of Open Access Journals (Sweden)

    Xiaotong Ye

    2017-10-01

    Full Text Available Porous Ti-6Al-4V scaffolds fabricated by means of selective laser melting (SLM, having controllable geometrical features and preferable mechanical properties, have been developed as a class of biomaterials that hold promising potential for bone repair. However, the inherent bio-inertness of the Ti-6Al-4V alloy as the matrix of the scaffolds results in a lack in the ability to stimulate bone ingrowth and regeneration. The aim of the present study was to develop a bioactive coating on the struts of SLM Ti-6Al-4V scaffolds in order to add the desired surface osteogenesis ability. Mesoporous bioactive glasses (MBGs coating was applied on the strut surfaces of the SLM Ti-6Al-4V scaffolds through spin coating, followed by a heat treatment. It was found that the coating could maintain the characteristic mesoporous structure and chemical composition of MBG, and establish good interfacial adhesion to the Ti-6Al-4V substrate. The compressive strength and pore interconnectivity of the scaffolds were not affected by the coating. Moreover, the results obtained from in vitro cell culture experiments demonstrated that the attachment, proliferation, and differentiation of human bone marrow stromal cells (hBMSCs on the MBG-coated Ti-6Al-4V scaffolds were improved as compared with those on the conventional bioactive glass (BG-coated Ti-6Al-4V scaffolds and bare-metal Ti-6Al-4V scaffolds. Our results demonstrated that the MBG coating by using the spinning coating method could be an effective approach to achieving enhanced surface biofunctionalization for SLM Ti-6Al-4V scaffolds.

  6. Improved surface bioactivity of stainless steel substrates using osteocalcin mimetic peptide

    International Nuclear Information System (INIS)

    Hosseini, Samaneh; Naderi-Manesh, Hossein; Vali, Hojatollah; Faghihi, Shahab

    2014-01-01

    calcium binding ability and used as stainless steel substrates coating. The osteocalcin mimetic peptide has ability to promote hydroxyapatite crystal formation on the substrates and increase surface bioactivity. - Highlights: • The effect of osteocalcin (OC) mimetic peptide as coating material is investigated. • The bioactivity is assessed by the ability of the substrates to form hydroxyapatite (HA). • It is demonstrated that OC-derived peptide promotes HA crystal nucleation and growth. • OC mimetic peptide promotes hard tissue regeneration as coating material

  7. Improved surface bioactivity of stainless steel substrates using osteocalcin mimetic peptide

    Energy Technology Data Exchange (ETDEWEB)

    Hosseini, Samaneh [Department of Nanobiotechnology, Faculty of Biological Sciences, Tarbiat Modares University, Tehran (Iran, Islamic Republic of); Tissue Engineering and Biomaterials Division, National Institute of Genetic Engineering and Biotechnology, Tehran 14965/161 (Iran, Islamic Republic of); Naderi-Manesh, Hossein, E-mail: naderman@modares.ac.ir [Department of Nanobiotechnology, Faculty of Biological Sciences, Tarbiat Modares University, Tehran (Iran, Islamic Republic of); Vali, Hojatollah [Department of Anatomy and Cell Biology, McGill University, 3640 University Street, Montréal, QC H3A 0C7 (Canada); Faghihi, Shahab, E-mail: sfaghihi@nigeb.ac.ir [Tissue Engineering and Biomaterials Division, National Institute of Genetic Engineering and Biotechnology, Tehran 14965/161 (Iran, Islamic Republic of)

    2014-02-14

    calcium binding ability and used as stainless steel substrates coating. The osteocalcin mimetic peptide has ability to promote hydroxyapatite crystal formation on the substrates and increase surface bioactivity. - Highlights: • The effect of osteocalcin (OC) mimetic peptide as coating material is investigated. • The bioactivity is assessed by the ability of the substrates to form hydroxyapatite (HA). • It is demonstrated that OC-derived peptide promotes HA crystal nucleation and growth. • OC mimetic peptide promotes hard tissue regeneration as coating material.

  8. Is There a Role for Bioactive Lipids in the Pathobiology of Diabetes Mellitus?

    Directory of Open Access Journals (Sweden)

    Undurti N. Das

    2017-08-01

    Full Text Available Inflammation, decreased levels of circulating endothelial nitric oxide (eNO and brain-derived neurotrophic factor (BDNF, altered activity of hypothalamic neurotransmitters (including serotonin and vagal tone and gut hormones, increased concentrations of free radicals, and imbalance in the levels of bioactive lipids and their pro- and anti-inflammatory metabolites have been suggested to play a role in diabetes mellitus (DM. Type 1 diabetes mellitus (type 1 DM is due to autoimmune destruction of pancreatic β cells because of enhanced production of IL-6 and tumor necrosis factor-α (TNF-α and other pro-inflammatory cytokines released by immunocytes infiltrating the pancreas in response to unknown exogenous and endogenous toxin(s. On the other hand, type 2 DM is due to increased peripheral insulin resistance secondary to enhanced production of IL-6 and TNF-α in response to high-fat and/or calorie-rich diet (rich in saturated and trans fats. Type 2 DM is also associated with significant alterations in the production and action of hypothalamic neurotransmitters, eNO, BDNF, free radicals, gut hormones, and vagus nerve activity. Thus, type 1 DM is because of excess production of pro-inflammatory cytokines close to β cells, whereas type 2 DM is due to excess of pro-inflammatory cytokines in the systemic circulation. Hence, methods designed to suppress excess production of pro-inflammatory cytokines may form a new approach to prevent both type 1 and type 2 DM. Roux-en-Y gastric bypass and similar surgeries ameliorate type 2 DM, partly by restoring to normal: gut hormones, hypothalamic neurotransmitters, eNO, vagal activity, gut microbiota, bioactive lipids, BDNF production in the gut and hypothalamus, concentrations of cytokines and free radicals that results in resetting glucose-stimulated insulin production by pancreatic β cells. Our recent studies suggested that bioactive lipids, such as arachidonic acid, eicosapentaneoic acid, and docosahexaenoic

  9. Incorporation of sol–gel bioactive glass into PLGA improves mechanical properties and bioactivity of composite scaffolds and results in their osteoinductive properties

    International Nuclear Information System (INIS)

    Filipowska, J; Tylko, G; Osyczka, A M; Pawlik, J; Cholewa-Kowalska, K; Laczka, M; Pamula, E; Niedzwiedzki, L; Szuta, M

    2014-01-01

    In this study, 3D porous bioactive composite scaffolds were produced and evaluated for their physico-chemical and biological properties. Polymer poly-L-lactide-co-glycolide (PLGA) matrix scaffolds were modified with sol–gel-derived bioactive glasses (SBGs) of CaO–SiO 2 –P 2 O 5 systems. We hypothesized that SBG incorporation into PLGA matrix would improve the chemical and biological activity of composite materials as well as their mechanical properties. We applied two bioactive glasses, designated as S2 or A2, differing in the content of SiO 2 and CaO (i.e. 80 mol% SiO 2 , 16 mol% CaO for S2 and 40 mol% SiO 2 , 52 mol% CaO for A2). The composites were characterized for their porosity, bioactivity, microstructure and mechanical properties. The osteoinductive properties of these composites were evaluated in human bone marrow stromal cell (hBMSC) cultures grown in either standard growth medium or treated with recombinant human bone morphogenetic protein-2 (rhBMP-2) or dexamethasone (Dex). After incubation in simulated body fluid, calcium phosphate precipitates formed inside the pores of both A2-PLGA and S2-PLGA scaffolds. The compressive strength of the latter was increased slightly compared to PLGA. Both composites promoted superior hBMSC attachment to the material surface and stimulated the expression of several osteogenic markers in hBMSC compared to cells grown on unmodified PLGA. There were also marked differences in the response of hBMSC to composite scaffolds, depending on chemical compositions of the scaffolds and culture treatments. Compared to silica-rich S2-PLGA, hBMSC grown on calcium-rich A2-PLGA were overall less responsive to rhBMP-2 or Dex and the osteoinductive properties of these A2-PLGA scaffolds seemed partially dependent on their ability to induce BMP signaling in untreated hBMSC. Thus, beyond the ability of currently studied composites to enhance hBMSC osteogenesis, it may become possible to modulate the osteogenic response of h

  10. Nano-Hydroxyapatite/Fluoridated and Unfluoridated Bioactive Glass Composites: Structural Analysis and Bioactivity Evaluation

    International Nuclear Information System (INIS)

    Batra, Uma; Kapoor, Seema; Sharma, J. D.

    2011-01-01

    Biphasic bioceramic composites containing nano-hydroxyapatite (HAP) and nanosized bioactive glasses have been prepared in the form of pellets and have been examined for the effects of bioglass concentrations and sintering temperature on the structural transformations and bioactivity behavior. Pure stoichiometric nano-HAP was synthesized using sol-gel technique. Two bioglasses synthesized in this work--fluoridated bioglass (Cao-P 2 O 5 -Na 2 O 3 -CaF 2 ) and unfluoridated bioglass (Cao-P 2 O 5 -Na 2 O 3 ) designated as FBG and UFBG respectively, were added to nano-HAP with concentrations of 5, 10, 12 and 15%. The average particle sizes of synthesized HAP and bioglasses were 23 nm and 35 nm, respectively. The pellets were sintered at four different temperatures i.e. 1000 deg. C, 1150 deg. C, 1250 deg. C and 1350 deg. C. The investigations involved study of structural and bioactivity behavior of green and sintered pellets and their deviations from original materials i.e. HAP, FBG and UFBG, using X-ray diffraction (XRD) and scanning electron microscopy (SEM). The phase composition of the sintered pellets was found to be non-stoichiometric HAP with α-TCP (tricalcium phosphate) and β-TCP. It was revealed from SEM images that bonding mechanism was mainly solid state sintering for all pellets sintered at 1000 deg. C and 1150 deg. C and also for pellets with lower concentrations of bioglass i.e. 5% and 10% sintered at 1250 deg. C. Partly liquid phase sintering was observed for pellets with higher bioglass concentrations of 12% and 15% sintered at 1250 deg. C and same behaviour was noted for pellets at all concentrations of bioglasses at 1350 deg. C. The sintered density, hardness and compression strength of pellets have been influenced both by the concentration of the bioglasses and sintering temperature. It was observed that the biological HAP layer formation was faster on the green pellets surface than on pure HAP and sintered pellets, showing higher bioactivity in the

  11. Bioactive Glasses: Where Are We and Where Are We Going?

    Directory of Open Access Journals (Sweden)

    Francesco Baino

    2018-03-01

    Full Text Available Bioactive glasses caused a revolution in healthcare and paved the way for modern biomaterial-driven regenerative medicine. The first 45S5 glass composition, invented by Larry Hench fifty years ago, was able to bond to living bone and to stimulate osteogenesis through the release of biologically-active ions. 45S5-based glass products have been successfully implanted in millions of patients worldwide, mainly to repair bone and dental defects and, over the years, many other bioactive glass compositions have been proposed for innovative biomedical applications, such as soft tissue repair and drug delivery. The full potential of bioactive glasses seems still yet to be fulfilled, and many of today’s achievements were unthinkable when research began. As a result, the research involving bioactive glasses is highly stimulating and requires a cross-disciplinary collaboration among glass chemists, bioengineers, and clinicians. The present article provides a picture of the current clinical applications of bioactive glasses, and depicts six relevant challenges deserving to be tackled in the near future. We hope that this work can be useful to both early-stage researchers, who are moving with their first steps in the world of bioactive glasses, and experienced scientists, to stimulate discussion about future research and discover new applications for glass in medicine.

  12. Bioactive Glasses: Where Are We and Where Are We Going?

    Science.gov (United States)

    Baino, Francesco; Hamzehlou, Sepideh; Kargozar, Saeid

    2018-03-19

    Bioactive glasses caused a revolution in healthcare and paved the way for modern biomaterial-driven regenerative medicine. The first 45S5 glass composition, invented by Larry Hench fifty years ago, was able to bond to living bone and to stimulate osteogenesis through the release of biologically-active ions. 45S5-based glass products have been successfully implanted in millions of patients worldwide, mainly to repair bone and dental defects and, over the years, many other bioactive glass compositions have been proposed for innovative biomedical applications, such as soft tissue repair and drug delivery. The full potential of bioactive glasses seems still yet to be fulfilled, and many of today's achievements were unthinkable when research began. As a result, the research involving bioactive glasses is highly stimulating and requires a cross-disciplinary collaboration among glass chemists, bioengineers, and clinicians. The present article provides a picture of the current clinical applications of bioactive glasses, and depicts six relevant challenges deserving to be tackled in the near future. We hope that this work can be useful to both early-stage researchers, who are moving with their first steps in the world of bioactive glasses, and experienced scientists, to stimulate discussion about future research and discover new applications for glass in medicine.

  13. Bioactive chromone constituents from Vitex negundo alleviate pain and inflammation

    Directory of Open Access Journals (Sweden)

    Khan A

    2017-12-01

    Full Text Available Ajmal Khan,1,2 Sadia Naz,1 Umar Farooq,1 Muhammad Shahid,3 Irfan Ullah,4 Iftikhar Ali,5 Abdur Rauf,6 Yahia Nasser Mabkhot7 1Department of Chemistry, COMSATS Institute of Information Technology, Abbottabad, Pakistan; 2University of Nizwa Chair of Oman’s Medicinal Plants and Marine Natural Products, University of Nizwa, Nizwa, Oman; 3Department of Pharmacy, Sarhad University of Science and Information Technology, 4Department of Pharmacy, University of Peshawar, Peshawar, 5Department of Chemistry, Karakoram International University, Gilgit-Baltistan, 6Department of Chemistry, University of Swabi, Khyber Pakhtunkhwa, Pakistan; 7Department of Chemistry, College of Science, King Saud University, Riyadh, Saudi Arabia Background: Vitex negundo L. has been widely studied for its beneficial effect in inflammatory and pain conditions. The present study describes the isolation of two new bioactive chromone constituents from V. negundo and their in vivo evaluation for anti-inflammatory and antinociceptive activities. Methods: Two new chromone derivatives, namely, methyl 3-(2-(5-hydroxy-6-methoxy-4-oxo-4H-chromen-2-ylethylbenzoate (1 and 3-(1-hydroxy-2-(5-hydroxy-6-methoxy-4-oxo-4H-chromen-2-ylethylbenzoic acid (2 were isolated from V. negundo and their structures were determined through various spectroscopic techniques including mass spectrometry, UV, IR, 1H NMR, 13C NMR, and two-dimensional-NMR like correlation spectroscopy and heteronuclear multiple bond correlation techniques. The isolated compounds (1–2 were tested for their prospective antinociceptive activity in acetic acid-induced abdominal constriction assay and anti-inflammatory activity in the carrageenan-induced paw edema assay in mice. Results: Significant attenuation (P<0.001 of tonic visceral nociception was demonstrated by compound 1 and 2 at doses of 50 and 100 mg/kg. At similar doses, these compounds (1–2 also showed potent amelioration (P<0.001 of carrageenan-induced paw swelling

  14. Screening for bioactivity of Mutinus elegans extracts

    Science.gov (United States)

    Gajendiran, A.; Cyriac, RE; Abraham, J.

    2017-11-01

    Mutinus elegans is a species of fungi that is commonly called as Elegant Stinkhorn. The aim of this study was to screen the crude extracts of the fungus for phytochemical analysis, antimicrobial activity, antioxidant assay and anticancer activity. Extraction of the fungal sample in Soxhlet apparatus was done with n-hexane and methanol as the solvent. Stock solutions of the crude methanol extract were prepared and used for microbiological assay. Thin layer chromatography was performed in order to determine the number of active components in n-hexane, and methanol solvent system for the fungus Mutinus elegans. Further, antioxidant assay was performed using DPPH radical scavenging assay. The fungal sample was then tested for cytotoxicity assay against MG63 osteosarcoma cell lines. The antimicrobial assay of Mutinus elegans extract exhibited activity against five pathogens. The zone of inhibition was measured with respect to standard antibiotics. Gas chromatography and Mass spectrometry (GC/MS analysis), revealed the presence of dibromo-tetradecan-1-ol-acetate, 2-myristynoyl-glycinamide, fumaric acid, and cyclohexylmethyldecyl ester compounds were presented in methanol and n-hexane extract of Mutinus elegans. The present study concludes the presence of bioactive compound in the extract which exhibited antimicrobial and antioxidant activity in Mutinus elegans.

  15. Triterpene Composition and Bioactivities of Centella asiatica

    Directory of Open Access Journals (Sweden)

    Uma Devi Palanisamy

    2011-01-01

    Full Text Available Leaves of Centella asiatica (Centella were analysed for their triterpene composition and bioactivity such as collagen enhancement, antioxidant, anticellulite and UV protection capacity properties. Triterpenes of Centella were measured using HPLC-PAD on an Excil ODS 5 mm (C18 column for the simultaneous determination of asiatic acid, madecassic acid, asiaticoside and madecassoside. Centella was found to contain significant amounts of madecassoside (3.10 ± 4.58 mg/mL and asiaticoside (1.97 ± 2.65 mg/mL, but was low in asiatic and madecassic acid. The highest collagen synthesis was found at 50 mg/mL of Centella extracts. The antioxidant activity of Centella (84% was compared to grape seed extract (83% and Vitamin C (88%. Its lipolytic activity was observed by the release of glycerol (115.9 µmol/L at 0.02% concentration. Centella extracts exhibited similar UV protection effect to OMC at 10% concentration. In view of these results, the potential application of Centella in food and pharmaceutical industries is now widely open.

  16. Bioactivities of Traditional Medicinal Plants in Alexandria.

    Science.gov (United States)

    Elansary, Hosam O; Szopa, Agnieszka; Kubica, Paweł; Ekiert, Halina; Ali, Hayssam M; Elshikh, Mohamed S; Abdel-Salam, Eslam M; El-Esawi, Mohamed; El-Ansary, Diaa O

    2018-01-01

    In traditional folklore, medicinal herbs play a vital role in the prevention and treatment of microbial diseases. In the present study, the phenolic profiles of the medicinal plants Asparagus aethiopicus L., Citrullus colocynthis L., Senna alexandrina L., Kalanchoe delagoensis L., Gasteria pillansii L., Cymbopogon citratus , Brassica juncea , and Curcuma longa L. were determined by high-performance liquid chromatography with a diode-array detector method. The results revealed rich sources of important compounds such as robinin in the fruits and leaves of A. aethiopicus ; caffeic acid in the tubers of A. aethiopicus and quercitrin in the leaves of G. pillansii . Further, relatively high antioxidant, antibacterial, and antifungal activities were observed in C. colocynthis fruit coat, S. alexandrina pods, and A. aethiopicus leaves, respectively. The relatively higher the bioactivities of plants extracts associated with the phenols in these plants, in particular, the more abundant the phenols. Therefore, it was concluded that the fruit coat of C. colocynthis , pods of S. alexandrina , and leaves of A. aethiopicus might be excellent sources of natural products. These plant extracts also have a wide spectrum of antimicrobial activities that could be used in the pharmaceutical industries and to control diseases.

  17. Radiation technology for immobilization of bioactive materials

    International Nuclear Information System (INIS)

    1988-12-01

    Within the framework of the Agency's coordinated research programme on ''Application of Radiation Technology in Immobilization of Bioactive Materials'', the third and final research coordination meeting was held at Beijing University, Beijing, People's Republic of China, 15-18 June 1987. The present publication compiles all presentations made at the meeting. Fundamental processes for the immobilization of enzymes, antibodies, cells and drugs were developed and established using gamma radiation, electron beams and plasma discharge. Applications of various biofunctional components, immobilized by radiation techniques in different processes, were studied. A range of backbone polymers has been examined together with various monomers. Coupling procedures have been developed which are relevant to our particular requirements. Enzymes of various types and characteristics have been immobilized with considerable efficiency. The immobilized biocatalysts have been shown to possess significant activity and retention of activity on storage. There appears to be a high degree of specificity associated with the properties of the immobilised biocatalysts, their activity and the ease of their preparation. Novel additives which lower the total radiation dose in grafting have been discovered and their value in immobilization processes assessed. Potential applications include: medical (diagnostic, therapeutic), and industrial processes (fermentation, bioseparation, etc.). Refs, figs and tabs

  18. Bioactivities of Traditional Medicinal Plants in Alexandria

    Directory of Open Access Journals (Sweden)

    Hosam O. Elansary

    2018-01-01

    Full Text Available In traditional folklore, medicinal herbs play a vital role in the prevention and treatment of microbial diseases. In the present study, the phenolic profiles of the medicinal plants Asparagus aethiopicus L., Citrullus colocynthis L., Senna alexandrina L., Kalanchoe delagoensis L., Gasteria pillansii L., Cymbopogon citratus, Brassica juncea, and Curcuma longa L. were determined by high-performance liquid chromatography with a diode-array detector method. The results revealed rich sources of important compounds such as robinin in the fruits and leaves of A. aethiopicus; caffeic acid in the tubers of A. aethiopicus and quercitrin in the leaves of G. pillansii. Further, relatively high antioxidant, antibacterial, and antifungal activities were observed in C. colocynthis fruit coat, S. alexandrina pods, and A. aethiopicus leaves, respectively. The relatively higher the bioactivities of plants extracts associated with the phenols in these plants, in particular, the more abundant the phenols. Therefore, it was concluded that the fruit coat of C. colocynthis, pods of S. alexandrina, and leaves of A. aethiopicus might be excellent sources of natural products. These plant extracts also have a wide spectrum of antimicrobial activities that could be used in the pharmaceutical industries and to control diseases.

  19. Bioactive Polymeric Nanoparticles for Periodontal Therapy.

    Science.gov (United States)

    Osorio, Raquel; Alfonso-Rodríguez, Camilo Andrés; Medina-Castillo, Antonio L; Alaminos, Miguel; Toledano, Manuel

    2016-01-01

    to design calcium and zinc-loaded bioactive and cytocompatible nanoparticles for the treatment of periodontal disease. PolymP-nActive nanoparticles were zinc or calcium loaded. Biomimetic calcium phosphate precipitation on polymeric particles was assessed after 7 days immersion in simulated body fluid, by scanning electron microscopy attached to an energy dispersive analysis system. Amorphous mineral deposition was probed by X-ray diffraction. Cell viability analysis was performed using oral mucosa fibroblasts by: 1) quantifying the liberated deoxyribonucleic acid from dead cells, 2) detecting the amount of lactate dehydrogenase enzyme released by cells with damaged membranes, and 3) by examining the cytoplasmic esterase function and cell membranes integrity with a fluorescence-based method using the Live/Dead commercial kit. Data were analyzed by Kruskal-Wallis and Mann-Whitney tests. Precipitation of calcium and phosphate on the nanoparticles surfaces was observed in calcium-loaded nanoparticles. Non-loaded nanoparticles were found to be non-toxic in all the assays, calcium and zinc-loaded particles presented a dose dependent but very low cytotoxic effect. The ability of calcium-loaded nanoparticles to promote precipitation of calcium phosphate deposits, together with their observed non-toxicity may offer new strategies for periodontal disease treatment.

  20. Beneficial Oral Biofilms as Smart Bioactive Interfaces

    Directory of Open Access Journals (Sweden)

    Beatrice Gutt

    2018-01-01

    Full Text Available Periodontitis is a very common health problem caused by formation of pathogenic bacterial biofilm that triggers inflammation resulting in either reversible gingivitis or irreversible periodontal hard and soft tissue damages, leading to loss of teeth when left untreated. Commensal bacteria play an important role in oral health in many aspects. Mainly by colonizing oral tissues, they (i contribute to maturation of immune response, and (ii foreclose attachment of pathobiont and, therefore, prevent from infection. The main goal of the study was to investigate if blocking of receptors on a commensal biofilm can prevent or reduce the attachment of pathogenic strains. To do so, biofilm produced by commensal Streptococcus sanguinis was treated with whole cell lysate of pathobionts Fusobacterium nucleatum or Porphyromonas gingivalis, followed by incubation with respective strain(s. The study revealed significant reduction in pathobiont adhesion to lysate-treated commensal biofilm. Therefore, adhesion of pathobionts onto the lysate-blocked biofilm was hindered; however, not completely eliminated supporting the idea that such approach in the oral cavity would benefit the production of a well-balanced and healthy bioactive interface.

  1. Bioactivities of Traditional Medicinal Plants in Alexandria

    Science.gov (United States)

    Szopa, Agnieszka; Kubica, Paweł; Ekiert, Halina; Elshikh, Mohamed S.; Abdel-Salam, Eslam M.; El-Ansary, Diaa O.

    2018-01-01

    In traditional folklore, medicinal herbs play a vital role in the prevention and treatment of microbial diseases. In the present study, the phenolic profiles of the medicinal plants Asparagus aethiopicus L., Citrullus colocynthis L., Senna alexandrina L., Kalanchoe delagoensis L., Gasteria pillansii L., Cymbopogon citratus, Brassica juncea, and Curcuma longa L. were determined by high-performance liquid chromatography with a diode-array detector method. The results revealed rich sources of important compounds such as robinin in the fruits and leaves of A. aethiopicus; caffeic acid in the tubers of A. aethiopicus and quercitrin in the leaves of G. pillansii. Further, relatively high antioxidant, antibacterial, and antifungal activities were observed in C. colocynthis fruit coat, S. alexandrina pods, and A. aethiopicus leaves, respectively. The relatively higher the bioactivities of plants extracts associated with the phenols in these plants, in particular, the more abundant the phenols. Therefore, it was concluded that the fruit coat of C. colocynthis, pods of S. alexandrina, and leaves of A. aethiopicus might be excellent sources of natural products. These plant extracts also have a wide spectrum of antimicrobial activities that could be used in the pharmaceutical industries and to control diseases. PMID:29636772

  2. δ-Peptides from RuAAC-Derived 1,5-Disubstituted Triazole Units

    KAUST Repository

    Johansson, Johan R.

    2014-02-14

    Non-natural peptides with structures and functions similar to natural peptides have emerged lately in biomedical as well as nanotechnological contexts. They are interesting for pharmaceutical applications since they can adopt structures with new targeting potentials and because they are generally not prone to degradation by proteases. We report here a new set of peptidomimetics derived from δ-peptides, consisting of n units of a 1,5-disubstituted 1,2,3-triazole amino acid (5Tzl). The monomer was prepared using ruthenium-catalyzed azide-alkyne cycloaddition (RuAAC) chemistry using [RuCl2Cp]x as the catalyst, allowing for simpler purification and resulting in excellent yields. This achiral monomer was used to prepare peptide oligomers that are water soluble independent of peptide chain length. Conformational analysis and structural investigations of the oligomers were performed by 2D NOESY NMR experiments, and by quantum chemical calculations using the ωB97X-D functional. These data indicate that several conformations may co-exist with slight energetic differences. Together with their increased hydrophilicity, this feature of homo-5Tzl may prove essential for mimicking natural peptides composed of α-amino acids, where the various secondary structures are achieved by side chain effects and not by the rigidity of the peptide backbone. The improved synthetic method allows for facile variation of the 5Tzl amino acid side chains, further increasing the versatility of these compounds. A new set of non-natural peptides composed of 1,5-disubstituted 1,2,3-triazole amino acids is presented. These peptides benefit from: a) modular synthesis of the monomers, allowing variation of the side chains; b) increased solubility of the oligomers in water, irrespective of peptide length; c) flexibility of the backbone allowing these foldamers to adopt several conformations. Copyright © 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

  3. Review of Pharmacological Effects of Antrodia camphorata and Its Bioactive Compounds

    Directory of Open Access Journals (Sweden)

    Madamanchi Geethangili

    2011-01-01

    Full Text Available Antrodia camphorata is a unique mushroom of Taiwan, which has been used as a traditional medicine for protection of diverse health-related conditions. In an effort to translate this Eastern medicine into Western-accepted therapy, a great deal of work has been carried out on A. camphorata. This review discusses the biological activities of the crude extracts and the main bioactive compounds of A. camphorata. The list of bioactivities of crude extracts is huge, ranging from anti-cancer to vasorelaxation and others. Over 78 compounds consisting of terpenoids, benzenoids, lignans, benzoquinone derivatives, succinic and maleic derivatives, in addition to polysaccharides have been identified. Many of these compounds were evaluated for biological activity. Many activities of crude extracts and pure compounds of A. camphorata against some major diseases of our time, and thus, a current review is of great importance. It is concluded that A. camphorata can be considered as an efficient alternative phytotherapeutic agent or a synergizer in the treatment of cancer and other immune-related diseases. However, clinical trails of human on A. camphorata extracts are limited and those of pure compounds are absent. The next step is to produce some medicines from A. camphorata, however, the production may be hampered by problems related to mass production.

  4. The pharmacokinetics and pharmacodynamics of progastrin-derived peptides

    DEFF Research Database (Denmark)

    Hansen, Carsten Palnaes

    2003-01-01

    The elimination of progastrin-derived peptides was a first-order process, also at supraphysiological concentrations in plasma. The site of extraction was dependent on the molecular size of the peptides and not on their bioactivity. Apart from the kidneys and brain, where the extraction...

  5. Tanzanian Botanical Derivatives in the Control of Malaria Vectors ...

    African Journals Online (AJOL)

    This paper report on assessment of the chemicals derived from Tanzanian botanical resource as a viable source of safe, environmentally friendly and low cost mosquitocidal agents, but has yet to be developed into simple blends and formulations to be used in malaria control campaigns. Selection of bioactive plant species ...

  6. Fabrication and in vitro evaluation of a sponge-like bioactive-glass/gelatin composite scaffold for bone tissue engineering

    Energy Technology Data Exchange (ETDEWEB)

    Nadeem, Danish [Biomaterials Engineering Group, School of Oral and Dental Sciences, University of Bristol, BS1 2LY (United Kingdom); Kiamehr, Mostafa [Biomaterials and Tissue Engineering Group, Leeds Dental Institute, University of Leeds, LS2 9LU (United Kingdom); Yang, Xuebin [Biomaterials and Tissue Engineering Group, Leeds Dental Institute, University of Leeds, LS2 9LU (United Kingdom); NIHR Leeds Musculoskeletal Biomedical Research Unit, Chapel Allerton Hospital, Leeds LS7 4SA (United Kingdom); Su, Bo, E-mail: b.su@bristol.ac.uk [Biomaterials Engineering Group, School of Oral and Dental Sciences, University of Bristol, BS1 2LY (United Kingdom)

    2013-07-01

    In this work a bioactive composite scaffold, comprised of bioactive-glass and gelatin, is introduced. Through direct foaming a sponge-like composite of a sol–gel derived bioactive-glass (70S30C; 70% SiO{sub 2}, 30% CaO) and porcine gelatin was developed for use as a biodegradable scaffold for bone tissue engineering. The composite was developed to provide a suitable alternative to synthetic polymer based scaffolds, allowing directed regeneration of bone tissue. The fabricated scaffold was characterised through X-ray microtomography, scanning electron and light microscopy demonstrating a three dimensionally porous and interconnected structure, with an average pore size (170 μm) suitable for successful cell proliferation and tissue ingrowth. Acellular bioactivity was assessed through apatite formation during submersion in simulated body fluid (SBF) whereby the rate and onset of apatite nucleation was found to be comparable to that of bioactive-glass. Modification of dehydrothermal treatment parameters induced varying degrees of crosslinking, allowing the degradation of the composite to be tailored to suit specific applications and establishing its potential for a wide range of applications. Use of genipin to supplement crosslinking by dehydrothermal treatment provided further means of modifying degradability. Biocompatibility of the composite was qualified through successful cultures of human dental pulp stem cells (HDPSCs) on samples of the composite scaffold. Osteogenic differentiation of HDPSCs and extracellular matrix deposition were confirmed through positive alkaline phosphatase staining and immunohistochemistry. - Highlights: ► Optimised composition and fabrication produced sponge-like porosity (pore size ∼ 170 μm). ► Maximum aqueous stability via dehydrothermal treatment at 145 °C, for 48 h ► Biocompatibility and osteogenic potential confirmed via successful HDPSC cultures. ► Minimal toxicity exhibited in optimally crosslinked samples (10 m

  7. Fabrication and in vitro evaluation of a sponge-like bioactive-glass/gelatin composite scaffold for bone tissue engineering

    International Nuclear Information System (INIS)

    Nadeem, Danish; Kiamehr, Mostafa; Yang, Xuebin; Su, Bo

    2013-01-01

    In this work a bioactive composite scaffold, comprised of bioactive-glass and gelatin, is introduced. Through direct foaming a sponge-like composite of a sol–gel derived bioactive-glass (70S30C; 70% SiO 2 , 30% CaO) and porcine gelatin was developed for use as a biodegradable scaffold for bone tissue engineering. The composite was developed to provide a suitable alternative to synthetic polymer based scaffolds, allowing directed regeneration of bone tissue. The fabricated scaffold was characterised through X-ray microtomography, scanning electron and light microscopy demonstrating a three dimensionally porous and interconnected structure, with an average pore size (170 μm) suitable for successful cell proliferation and tissue ingrowth. Acellular bioactivity was assessed through apatite formation during submersion in simulated body fluid (SBF) whereby the rate and onset of apatite nucleation was found to be comparable to that of bioactive-glass. Modification of dehydrothermal treatment parameters induced varying degrees of crosslinking, allowing the degradation of the composite to be tailored to suit specific applications and establishing its potential for a wide range of applications. Use of genipin to supplement crosslinking by dehydrothermal treatment provided further means of modifying degradability. Biocompatibility of the composite was qualified through successful cultures of human dental pulp stem cells (HDPSCs) on samples of the composite scaffold. Osteogenic differentiation of HDPSCs and extracellular matrix deposition were confirmed through positive alkaline phosphatase staining and immunohistochemistry. - Highlights: ► Optimised composition and fabrication produced sponge-like porosity (pore size ∼ 170 μm). ► Maximum aqueous stability via dehydrothermal treatment at 145 °C, for 48 h ► Biocompatibility and osteogenic potential confirmed via successful HDPSC cultures. ► Minimal toxicity exhibited in optimally crosslinked samples (10 m

  8. Synchrotron X-ray Absorption and In Vitro Bioactivity of Magnetic Macro/Mesoporous Bioactive Glasses

    Directory of Open Access Journals (Sweden)

    Thanida Charoensuk

    2015-12-01

    Full Text Available Iron oxides in macro/mesoporous bioactive glasses were characterized by synchrotron X-ray absorption near edge structure (XANES spectroscopy. This magnetic phase was introduced by adding Fe(NO33 9H2O during the sol-gel synthesis. The obtained bioactive glass scaffolds exhibited superparamagnetism, in which the magnetization was increased with the increase in the Fe molar ratio from 10 to 20%. The linear combination fits of the XANES spectra indicated that the increase in the Fe molar ratio to 20% enhanced the γ-Fe2O3 formation at the expense of the α- Fe2O3 phase. This variation also promoted the formation of fine-grained bone-like apatites on the surface of the scaffolds in the in vitro test. The apatite growth between three and seven days was confirmed by the changing elemental compositions. However, the highest magnetic proportion led to the distortion of the skeleton walls and the collapse of the porous networks.

  9. Bioactive phenolic acids from Scorzonera radiata Fisch.

    Directory of Open Access Journals (Sweden)

    N Tsevegsuren

    2014-09-01

    Full Text Available Chromatographic separation of the crude extract obtained from the aerial parts of the Mongolian medicinal plant Scorzonera radiata yielded five new dihydrostilbenes [4], two new flavonoids, one new quinic acid derivative, as well as twenty known compounds including eight quinic acid derivatives, four flavonoids, two coumarins, five simple benzoic acids, and one monoterpene glycoside. We present here results on isolation and structural identification some active phenolic compounds from the Scorzonera radiata - eight quinic acid derivatives (quinic acid, 4,5-dicaffeoylquinic acid, 4,5-dicaffeoyl-epi-quinic acid, 3,5-dicaffeoylquinic acid, 3,5-dicaffeoyl-epi-quinic acid, chlorogenic acid, 5-p-coumaroylquinic acid (trans, 5-p-coumaroylquinic acid (cis. Quinic acid derivatives exhibited antioxidative activity.DOI: http://dx.doi.org/10.5564/mjc.v12i0.177 Mongolian Journal of Chemistry Vol.12 2011: 78-84

  10. Chemical composition and bioactive compounds of garlic (Allium sativum L.) as affected by pre- and post-harvest conditions: A review.

    Science.gov (United States)

    Martins, Natália; Petropoulos, Spyridon; Ferreira, Isabel C F R

    2016-11-15

    Garlic (Allium sativum L.) is considered one of the twenty most important vegetables, with various uses throughout the world, either as a raw vegetable for culinary purposes, or as an ingredient of traditional and modern medicine. Furthermore, it has also been proposed as one of the richest sources of total phenolic compounds, among the usually consumed vegetables, and has been highly ranked regarding its contribution of phenolic compounds to human diet. This review aims to examine all the aspects related with garlic chemical composition and quality, focusing on its bioactive properties. A particular emphasis is given on the organosulfur compounds content, since they highly contribute to the effective bioactive properties of garlic, including its derived products. The important effects of pre-harvest (genotype and various cultivation practices) and post-harvest conditions (storage conditions and processing treatments) on chemical composition and, consequently, bioactive potency of garlic are also discussed. Copyright © 2016 Elsevier Ltd. All rights reserved.

  11. Phosphate glass fibre scaffolds: Tailoring of the properties and enhancement of the bioactivity through mesoporous glass particles.

    Science.gov (United States)

    Novajra, G; Boetti, N G; Lousteau, J; Fiorilli, S; Milanese, D; Vitale-Brovarone, C

    2016-10-01

    Novel bone glass fibre scaffolds were developed by thermally bonding phosphate glass fibres belonging to the P2O5-CaO-Na2O-SiO2-MgO-K2O-TiO2 system (TiPS2.5 glass). Scaffolds with fibres of 85 or 110μm diameter were fabricated, showing compressive strength in the range of 2-3.5MPa, comparable to that of the trabecular bone. The effect of different thermal treatments and fibre diameters and length on the final scaffold structure was investigated by means of micro-CT analysis. The change of the sintering time from 30 to 60min led to a decrease in the scaffold overall porosity from 58 to 21vol.% for the 85μm fibre scaffold and from 50 to 40vol.% when increasing the sintering temperature from 490 to 500°C for the 110μm fibre scaffold. The 85μm fibres resulted in an increase of the scaffold overall porosity, increased pore size and lower trabecular thickness; the use of different fibre diameters allowed the fabrication of a scaffold showing a porosity gradient. In order to impart bioactive properties to the scaffold, for the first time in the literature the introduction in these fibre scaffolds of a bioactive phase, a melt-derived bioactive glass (CEL2) powder or spray-dried mesoporous bioactive glass particles (SD-MBG) was investigated. The scaffold bioactivity was assessed through soaking in simulated body fluid. CEL2/glass fibre scaffold did not show promising results due to particle detachment from the fibres during soaking in simulated body fluid. Instead the use of mesoporous bioactive powders showed to be an effective way to impart bioactivity to the scaffold and could be further exploited in the future through the ability of mesoporous particles to act as systems for the controlled release of drugs. Copyright © 2016 Elsevier B.V. All rights reserved.

  12. Global Derivatives

    DEFF Research Database (Denmark)

    Andersen, Torben Juul

    approaches to dealing in the global business environment." - Sharon Brown-Hruska, Commissioner, Commodity Futures Trading Commission, USA. "This comprehensive survey of modern risk management using derivative securities is a fine demonstration of the practical relevance of modern derivatives theory to risk......" provides comprehensive coverage of different types of derivatives, including exchange traded contracts and over-the-counter instruments as well as real options. There is an equal emphasis on the practical application of derivatives and their actual uses in business transactions and corporate risk...... management situations. Its key features include: derivatives are introduced in a global market perspective; describes major derivative pricing models for practical use, extending these principles to valuation of real options; practical applications of derivative instruments are richly illustrated...

  13. Biotransformation and bioactivation reactions - 2016 literature highlights.

    Science.gov (United States)

    Khojasteh, S Cyrus; Rietjens, Ivonne M C M; Dalvie, Deepak; Miller, Grover

    2017-08-01

    We are pleased to present a second annual issue highlighting a previous year's literature on biotransformation and bioactivation. Each contributor to this issue worked independently to review the articles published in 2016 and proposed three to four articles, which he or she believed would be of interest to the broader research community. In each synopsis, the contributing author summarized the procedures, analyses and conclusions as described in the original manuscripts. In the commentary sections, our authors offer feedback and highlight aspects of the work that may not be apparent from an initial reading of the article. To be fair, one should still read the original article to gain a more complete understanding of the work conducted. Most of the articles included in this review were published in Drug Metabolism and Disposition or Chemical Research in Toxicology, but attempts were made to seek articles in 25 other journals. Importantly, these articles are not intended to represent a consensus of the best papers of the year, as we did not want to make any arbitrary standards for this purpose, but rather they were chosen by each author for their notable findings and descriptions of novel metabolic pathways or biotransformations. I am pleased that Drs. Rietjens and Dalvie have again contributed to this annual review. We would like to welcome Grover P Miller as an author for this year's issue, and we thank Tom Baillie for his contributions to last year's edition. We have intentionally maintained a balance of authors such that two come from an academic setting and two come from industry. Finally, please drop us a note if you find this review helpful. We would be pleased to hear your opinions of our commentary, and we extend an invitation to anyone who would like to contribute to a future edition of this review. This article is dedicated to Professor Thomas Baillie for his exceptional contributions to the field of drug metabolism.

  14. Porous surface modified bioactive bone cement for enhanced bone bonding.

    Directory of Open Access Journals (Sweden)

    Qiang He

    Full Text Available Polymethylmethacrylate bone cement cannot provide an adhesive chemical bonding to form a stable cement-bone interface. Bioactive bone cements show bone bonding ability, but their clinical application is limited because bone resorption is observed after implantation. Porous polymethylmethacrylate can be achieved with the addition of carboxymethylcellulose, alginate and gelatin microparticles to promote bone ingrowth, but the mechanical properties are too low to be used in orthopedic applications. Bone ingrowth into cement could decrease the possibility of bone resorption and promote the formation of a stable interface. However, scarce literature is reported on bioactive bone cements that allow bone ingrowth. In this paper, we reported a porous surface modified bioactive bone cement with desired mechanical properties, which could allow for bone ingrowth.The porous surface modified bioactive bone cement was evaluated to determine its handling characteristics, mechanical properties and behavior in a simulated body fluid. The in vitro cellular responses of the samples were also investigated in terms of cell attachment, proliferation, and osteoblastic differentiation. Furthermore, bone ingrowth was examined in a rabbit femoral condyle defect model by using micro-CT imaging and histological analysis. The strength of the implant-bone interface was also investigated by push-out tests.The modified bone cement with a low content of bioactive fillers resulted in proper handling characteristics and adequate mechanical properties, but slightly affected its bioactivity. Moreover, the degree of attachment, proliferation and osteogenic differentiation of preosteoblast cells was also increased. The results of the push-out test revealed that higher interfacial bonding strength was achieved with the modified bone cement because of the formation of the apatite layer and the osseointegration after implantation in the bony defect.Our findings suggested a new bioactive

  15. Synthetic Peptides Derived from Bovine Lactoferricin Exhibit Antimicrobial Activity against E. coli ATCC 11775, S. maltophilia ATCC 13636 and S. enteritidis ATCC 13076

    Directory of Open Access Journals (Sweden)

    Nataly De Jesús Huertas Méndez

    2017-03-01

    Full Text Available Linear, dimeric, tetrameric, and cyclic peptides derived from lactoferricin B–containing non-natural amino acids and the RWQWR motif were synthesized, purified, and characterized using RP-HPLC, MALDI-TOF mass spectrometry, and circular dichroism. The antibacterial activity of peptides against Escherichia coli ATCC 11775, Stenotrophomonas maltophilia ATCC 13636, and Salmonella enteritidis ATCC 13076 was evaluated. The minimum inhibitory concentration (MIC and minimum bactericidal concentration (MBC were determined. The synthetic bovine lactoferricin exhibited antibacterial activity against E. coli ATCC 11775 and S. enteritidis ATCC 13076. The dimeric peptide (RRWQWR2K-Ahx exhibited the highest antibacterial activity against the tested bacterial strain. The monomeric, cyclic, tetrameric, and palindromic peptides containing the RWQWR motif exhibited high and specific activity against E. coli ATCC 11775. The results suggest that short peptides derived from lactoferricin B could be considered as potential candidates for the development of antibacterial agents against infections caused by E. coli.

  16. Synthetic Peptides Derived from Bovine Lactoferricin Exhibit Antimicrobial Activity against E. coli ATCC 11775, S. maltophilia ATCC 13636 and S. enteritidis ATCC 13076.

    Science.gov (United States)

    Huertas Méndez, Nataly De Jesús; Vargas Casanova, Yerly; Gómez Chimbi, Anyelith Katherine; Hernández, Edith; Leal Castro, Aura Lucia; Melo Diaz, Javier Mauricio; Rivera Monroy, Zuly Jenny; García Castañeda, Javier Eduardo

    2017-03-12

    Linear, dimeric, tetrameric, and cyclic peptides derived from lactoferricin B-containing non-natural amino acids and the RWQWR motif were synthesized, purified, and characterized using RP-HPLC, MALDI-TOF mass spectrometry, and circular dichroism. The antibacterial activity of peptides against Escherichia coli ATCC 11775, Stenotrophomonas maltophilia ATCC 13636, and Salmonella enteritidis ATCC 13076 was evaluated. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) were determined. The synthetic bovine lactoferricin exhibited antibacterial activity against E. coli ATCC 11775 and S. enteritidis ATCC 13076. The dimeric peptide (RRWQWR)₂K-Ahx exhibited the highest antibacterial activity against the tested bacterial strain. The monomeric, cyclic, tetrameric, and palindromic peptides containing the RWQWR motif exhibited high and specific activity against E. coli ATCC 11775. The results suggest that short peptides derived from lactoferricin B could be considered as potential candidates for the development of antibacterial agents against infections caused by E. coli .

  17. Fabrication and characterization of strontium incorporated 3-D bioactive glass scaffolds for bone tissue from biosilica

    Energy Technology Data Exchange (ETDEWEB)

    Özarslan, Ali Can, E-mail: alicanozarslan@gmail.com; Yücel, Sevil, E-mail: syucel@yildiz.edu.tr

    2016-11-01

    Bioactive glass scaffolds that contain silica are high viable biomaterials as bone supporters for bone tissue engineering due to their bioactive behaviour in simulated body fluid (SBF). In the human body, these materials help inorganic bone structure formation due to a combination of the particular ratio of elements such as silicon (Si), calcium (Ca), sodium (Na) and phosphorus (P), and the doping of strontium (Sr) into the scaffold structure increases their bioactive behaviour. In this study, bioactive glass scaffolds were produced by using rice hull ash (RHA) silica and commercial silica based bioactive glasses. The structural properties of scaffolds such as pore size, porosity and also the bioactive behaviour were investigated. The results showed that undoped and Sr-doped RHA silica-based bioactive glass scaffolds have better bioactivity than that of commercial silica based bioactive glass scaffolds. Moreover, undoped and Sr-doped RHA silica-based bioactive glass scaffolds will be able to be used instead of undoped and Sr-doped commercial silica based bioactive glass scaffolds for bone regeneration applications. Scaffolds that are produced from undoped or Sr-doped RHA silica have high potential to form new bone for bone defects in tissue engineering. - Highlights: • Production of 3-D bioactive glass scaffolds from different silica sources • The effect of biosilica from rice hull ash on the bioactive glass scaffold • Sr additive impact on the bioactivity and biodegradability properties of scaffolds.

  18. Physical, bioactive and sensory quality parameters of reduced sugar chocolates formulated with natural sweeteners as sucrose alternatives.

    Science.gov (United States)

    Belščak-Cvitanović, Ana; Komes, Draženka; Dujmović, Marko; Karlović, Sven; Biškić, Matija; Brnčić, Mladen; Ježek, Damir

    2015-01-15

    In this study, sugar alcohols, dietary fibers, syrups and natural sweeteners were used as sucrose alternatives in the production of reduced sugar chocolates (50% of cocoa parts) with enhanced bioactive profile. Formulated chocolates were evaluated for their physical (particle size distribution, texture) and sensory properties, sugar composition, polyphenolic compounds content and antioxidant capacity. All produced reduced sugar chocolates ensured >20% lower calorific value than conventional chocolate (prepared with sucrose). Formulated chocolates containing stevia leaves and peppermint exhibited the best sensory properties (especially with regard to mouthfeel, sweetness and herbal aroma), as well as the highest polyphenolic content and antioxidant capacity. Particle size and hardness of chocolates increased in comparison to conventional chocolate, in particular when the combination of fructose and isomalt or lactitol was used. The bioactive profile of produced chocolates was enriched with phenolic acids, flavone (luteolin and apigenin) and flavonol (quercetin) derivatives, which were not identified in control chocolate. Copyright © 2014 Elsevier Ltd. All rights reserved.

  19. Antioxidant capacity and bioactive compounds of four Brazilian native fruits.

    Science.gov (United States)

    Denardin, Cristiane C; Hirsch, Gabriela E; da Rocha, Ricardo F; Vizzotto, Márcia; Henriques, Amélia T; Moreira, José C F; Guma, Fátima T C R; Emanuelli, Tatiana

    2015-09-01

    The purpose of this study was to evaluate the bioactive compounds and antioxidant activity of extracts from araçá (Psidium cattleianum), butiá (Butia eriospatha), and pitanga (Eugenia uniflora) fruits with different flesh colors (i.e., purple, red, and orange), and blackberries (Rubus sp.; cv. Xavante and Cherokee) collected in the southern region of Brazil. The content of ascorbic acid, total carotenoids, and phenolics were determined. The profile of the phenolic compounds was assessed by high-performance liquid chromatography combined with diode array detection (HPLC-DAD). The antioxidant activity was determined using the ferric-reducing antioxidant power (FRAP) assay, 2,2-diphenyl-2-picrylhydrazyl hydrate (DPPH) assay, total reactive antioxidant potential (TRAP) assay, and total antioxidant reactivity (TAR) assay. The Xavante blackberry and purple-fleshed pitanga showed the highest total phenolic content [816.50 mg gallic acid equivalents (GAE)/100g and 799.80 mg GAE/100g, respectively]. The araçá and red-fleshed pitanga showed the highest carotenoid content (6.27 ug β-carotene/g and 5.86 ug β-carotene/g, respectively). The fruits contained several phenolic compounds such as quercetin derivatives, quercitrin, isoquercitrin, and cyanidin derivatives, which may contribute differentially to the antioxidant capacity. The highest scavenging activity in the DPPH assay was found for purple-fleshed pitanga (IC 50 36.78 mg/L), blackberries [IC 50 44.70 (Xavante) and IC 50 78.25 mg/L (Cherokee)], and araçá (IC 50 48.05 mg/L), which also showed the highest FRAP, followed by orange- and red-fleshed pitanga. Our results revealed that some fruits grown in southern Brazil such as purple-fleshed pitanga, blackberries, and araçá are rich sources of phenolic compounds and have great antioxidant activity. Copyright © 2015. Published by Elsevier B.V.

  20. Advances in Microalgae-Derived Phytosterols for Functional Food and Pharmaceutical Applications.

    Science.gov (United States)

    Luo, Xuan; Su, Peng; Zhang, Wei

    2015-07-09

    Microalgae contain a variety of bioactive lipids with potential applications in aquaculture feed, biofuel, food and pharmaceutical industries. While microalgae-derived polyunsaturated fatty acid (PUFA) and their roles in promoting human health have been extensively studied, other lipid types from this resource, such as phytosterols, have been poorly explored. Phytosterols have been used as additives in many food products such as spread, dairy products and salad dressing. This review focuses on the recent advances in microalgae-derived phytosterols with functional bioactivities and their potential applications in functional food and pharmaceutical industries. It highlights the importance of microalgae-derived lipids other than PUFA for the development of an advanced microalgae industry.

  1. Financial Derivatives

    DEFF Research Database (Denmark)

    Wigan, Duncan

    2013-01-01

    Contemporary derivatives mark the development of capital and constitute a novel form of ownership. By reconfiguring the temporal, spatial and legal character of ownership derivatives present a substantive challenge to the tax collecting state. While fiscal systems are nationally bounded...... and inherently static, capital itself is unprecedentedly mobile, fluid and fungible. As such derivatives raise the specter of ‘financial weapons of mass destruction’....

  2. Financial Derivatives

    OpenAIRE

    Janečková, Alena

    2011-01-01

    1 Abstract/ Financial derivatives The purpose of this thesis is to provide an introduction to financial derivatives which has been, from the legal perspective, described in a not satisfactory manner as quite little literature that can be found about this topic. The main objectives of this thesis are to define the term "financial derivatives" and its particular types and to analyse legal nature of these financial instruments. The last objective is to try to draft future law regulation of finan...

  3. [Cytocompatibility of two porous bioactive glass-ceramic in vitro].

    Science.gov (United States)

    Zhang, Yan; Jiang, Xinquan; Zhang, Xiuli; Wang, Deping; Zhen, Lei

    2013-06-01

    To compare the cytocompatibility of two kinds porous bioactive glass-ceramic made by same raw materials. Apatite/wollastonite bioactive glass-ceramic (4006) were prepared by sol-gel method, and bioactive glass (45S5) were prepared by melting method. Bone marrow stromal cells (BMSCs) were cultivated, differentiated and proliferated into osteoblasts, from a rabbit's marrow in the differentiatiofn culture medium with active function. The viability of BMSCs cultivated with extraction of these two kinds of biomaterial, which could represent the cytotoxicity effect of 4006 and 45S5 against BMSCs, was evaluated by the MTp assay. BMSCs were seeded and cocultivated with two kinds of biomaterial scaffolds respectively in vitro. The proliferation and biological properties of cells adhered to scaffolds were observed by inverted phase contrast microscope, scanning electron microscope (SEM), and environmental scanning electron microscope (ESEM), and a suitable cell amount for seeding on the scaffold was searched. There was no difference on the viability of BMSCs only cultured for one day by complete extract of 4006 and culture medium (P>0.05), but there was significant difference between them when the cells had been cultured for 3 days(Pglass-ceramic has good bioactivity and cytocompatibility. Therefore, it may have the potential to be a new cell vehicle for bone tissue engineering. And the suitable seeding cell amount of apatite/wollastonite bioactive glass-ceramic should be 2x10(7) cells.mL-1 or even more than that.

  4. Plant proteases for bioactive peptides release: A review.

    Science.gov (United States)

    Mazorra-Manzano, M A; Ramírez-Suarez, J C; Yada, R Y

    2017-04-10

    Proteins are a potential source of health-promoting biomolecules with medical, nutraceutical, and food applications. Nowadays, bioactive peptides production, its isolation, characterization, and strategies for its delivery to target sites are a matter of intensive research. In vitro and in vivo studies regarding the bioactivity of peptides has generated strong evidence of their health benefits. Dairy proteins are considered the richest source of bioactive peptides, however proteins from animal and vegetable origin also have been shown to be important sources. Enzymatic hydrolysis has been the process most commonly used for bioactive peptide production. Most commercial enzymatic preparations frequently used are from animal (e.g., trypsin and pepsin) and microbial (e.g., Alcalase® and Neutrase®) sources. Although the use of plant proteases is still relatively limited to papain and bromelain from papaya and pineapple, respectively, the application of new plant proteases is increasing. This review presents the latest knowledge in the use and diversity of plant proteases for bioactive peptides release from food proteins including both available commercial plant proteases as well as new potential plant sources. Furthermore, the properties of peptides released by plant proteases and health benefits associated in the control of disorders such as hypertension, diabetes, obesity, and cancer are reviewed.

  5. Sodium Is Not Essential for High Bioactivity of Glasses

    Science.gov (United States)

    Chen, Xiaojing; Chen, Xiaohui; Brauer, Delia S.; Wilson, Rory M.; Law, Robert V.; Hill, Robert G.; Karpukhina, Natalia

    2017-01-01

    This study aims to demonstrate that excellent bioactivity of glass can be achieved without the presence of an alkali metal component in glass composition. In vitro bioactivity of two sodium-free glasses based on the quaternary system SiO2-P2O5-CaO-CaF2 with 0 and 4.5 mol% CaF2 content was investigated and compared with the sodium containing glasses with equivalent amount of CaF2. The formation of apatite after immersion in Tris buffer was followed by Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), 31P and 19F solid state MAS-NMR. The dissolution study was completed by ion release measurements in Tris buffer. The results show that sodium free bioactive glasses formed apatite at 3 hours of immersion in Tris buffer, which is as fast as the corresponding sodium containing composition. This signifies that sodium is not an essential component in bioactive glasses and it is possible to make equally degradable bioactive glasses with or without sodium. The results presented here also emphasize the central role of the glass compositions design which is based on understanding of structural role of components and/or predicting the network connectivity of glasses. PMID:29271977

  6. Sources and Bioactive Properties of Conjugated Dietary Fatty Acids.

    Science.gov (United States)

    Hennessy, Alan A; Ross, Paul R; Fitzgerald, Gerald F; Stanton, Catherine

    2016-04-01

    The group of conjugated fatty acids known as conjugated linoleic acid (CLA) isomers have been extensively studied with regard to their bioactive potential in treating some of the most prominent human health malignancies. However, CLA isomers are not the only group of potentially bioactive conjugated fatty acids currently undergoing study. In this regard, isomers of conjugated α-linolenic acid, conjugated nonadecadienoic acid and conjugated eicosapentaenoic acid, to name but a few, have undergone experimental assessment. These studies have indicated many of these conjugated fatty acid isomers commonly possess anti-carcinogenic, anti-adipogenic, anti-inflammatory and immune modulating properties, a number of which will be discussed in this review. The mechanisms through which these bioactivities are mediated have not yet been fully elucidated. However, existing evidence indicates that these fatty acids may play a role in modulating the expression of several oncogenes, cell cycle regulators, and genes associated with energy metabolism. Despite such bioactive potential, interest in these conjugated fatty acids has remained low relative to the CLA isomers. This may be partly attributed to the relatively recent emergence of these fatty acids as bioactives, but also due to a lack of awareness regarding sources from which they can be produced. In this review, we will also highlight the common sources of these conjugated fatty acids, including plants, algae, microbes and chemosynthesis.

  7. Bioinformatics approaches for identifying new therapeutic bioactive peptides in food

    Directory of Open Access Journals (Sweden)

    Nora Khaldi

    2012-10-01

    Full Text Available ABSTRACT:The traditional methods for mining foods for bioactive peptides are tedious and long. Similar to the drug industry, the length of time to identify and deliver a commercial health ingredient that reduces disease symptoms can take anything between 5 to 10 years. Reducing this time and effort is crucial in order to create new commercially viable products with clear and important health benefits. In the past few years, bioinformatics, the science that brings together fast computational biology, and efficient genome mining, is appearing as the long awaited solution to this problem. By quickly mining food genomes for characteristics of certain food therapeutic ingredients, researchers can potentially find new ones in a matter of a few weeks. Yet, surprisingly, very little success has been achieved so far using bioinformatics in mining for food bioactives.The absence of food specific bioinformatic mining tools, the slow integration of both experimental mining and bioinformatics, and the important difference between different experimental platforms are some of the reasons for the slow progress of bioinformatics in the field of functional food and more specifically in bioactive peptide discovery.In this paper I discuss some methods that could be easily translated, using a rational peptide bioinformatics design, to food bioactive peptide mining. I highlight the need for an integrated food peptide database. I also discuss how to better integrate experimental work with bioinformatics in order to improve the mining of food for bioactive peptides, therefore achieving a higher success rates.

  8. Bioactive carbon-PEEK composites prepared by chemical surface treatment.

    Science.gov (United States)

    Miyazaki, Toshiki; Matsunami, Chisato; Shirosaki, Yuki

    2017-01-01

    Polyetheretherketone (PEEK) has attracted much attention as an artificial intervertebral spacer for spinal reconstruction. Furthermore, PEEK plastic reinforced with carbon fiber has twice the bending strength of pure PEEK. However, the PEEK-based materials do not show ability for direct bone bonding, i.e., bioactivity. Although several trials have been conducted for enabling PEEK with bioactivity, few studies have reported on bioactive surface modification of carbon-PEEK composites. In the present study, we attempted the preparation of bioactive carbon-PEEK composites by chemical treatments with H 2 SO 4 and CaCl 2 . Bioactivity was evaluated by in vitro apatite formation in simulated body fluid (SBF). The apatite formation on the carbon-PEEK composite was compared with that of pure PEEK. Both pure PEEK and carbon-PEEK composite formed the apatite in SBF when they were treated with H 2 SO 4 and CaCl 2 ; the latter showed higher apatite-forming ability than the former. It is conjectured that many functional groups able to induce the apatite nucleation, such as sulfo and carboxyl groups, are incorporated into the dispersed carbon phase in the carbon-PEEK composites. Copyright © 2016 Elsevier B.V. All rights reserved.

  9. TRIS buffer in simulated body fluid distorts the assessment of glass-ceramic scaffold bioactivity.

    Science.gov (United States)

    Rohanová, Dana; Boccaccini, Aldo Roberto; Yunos, Darmawati Mohamad; Horkavcová, Diana; Březovská, Iva; Helebrant, Aleš

    2011-06-01

    The paper deals with the characterisation of the bioactive phenomena of glass-ceramic scaffold derived from Bioglass® (containing 77 wt.% of crystalline phases Na(2)O·2CaO·3SiO(2) and CaO·SiO(2) and 23 wt.% of residual glass phase) using simulated body fluid (SBF) buffered with tris-(hydroxymethyl) aminomethane (TRIS). A significant effect of the TRIS buffer on glass-ceramic scaffold dissolution in SBF was detected. To better understand the influence of the buffer, the glass-ceramic scaffold was exposed to a series of in vitro tests using different media as follows: (i) a fresh liquid flow of SBF containing tris (hydroxymethyl) aminomethane; (ii) SBF solution without TRIS buffer; (iii) TRIS buffer alone; and (iv) demineralised water. The in vitro tests were provided under static and dynamic arrangements. SBF buffered with TRIS dissolved both the crystalline and residual glass phases of the scaffold and a crystalline form of hydroxyapatite (HAp) developed on the scaffold surface. In contrast, when TRIS buffer was not present in the solutions only the residual glassy phase dissolved and an amorphous calcium phosphate (Ca-P) phase formed on the scaffold surface. It was confirmed that the TRIS buffer primarily dissolved the crystalline phase of the glass-ceramic, doubled the dissolving rate of the scaffold and moreover supported the formation of crystalline HAp. This significant effect of the buffer TRIS on bioactive glass-ceramic scaffold degradation in SBF has not been demonstrated previously and should be considered when analysing the results of SBF immersion bioactivity tests of such systems. Copyright © 2011 Acta Materialia Inc. Published by Elsevier Ltd. All rights reserved.

  10. Dextran derivatives modulate collagen matrix organization in dermal equivalent.

    Science.gov (United States)

    Frank, Laetitia; Lebreton-Decoster, Corinne; Godeau, Gaston; Coulomb, Bernard; Jozefonvicz, Jacqueline

    2006-01-01

    Dextran derivatives can protect heparin binding growth factor implied in wound healing, such as transforming growth factor-beta1 (TGF-beta1) and fibroblast growth factor-2 (FGF-2). The first aim of this study was to investigate the effect of these compounds on human dermal fibroblasts in culture with or without TGF-beta1. Several dextran derivatives obtained by substitution of methylcarboxylate (MC), benzylamide (B) and sulphate (Su) groups were used to determine the effects of each compound on fibroblast growth in vitro. The data indicate that sulphate groups are essential to act on the fibroblast proliferation. The dextran derivative LS21 DMCBSu has been chosen to investigate its effect on dermal wound healing process. Fibroblasts cultured in collagenous matrices named dermal equivalent were treated with the bioactive polymer alone or associated to TGF-beta1 or FGF-2. Cross-sections of dermal equivalent observed by histology or immunohistochemistry, demonstrated that the bioactive polymer accelerates the collagen matrices organization and stimulates the human type-III collagen expression. This bioactive polymer induces apoptosis of myofibroblast, property which may be beneficial in treatment of hypertrophic scar. Culture media analyzed by zymography and Western blot showed that this polymer significantly increases the secretion of zymogen and active form of matrix metalloproteinase-2 (MMP-2), involved in granulation tissue formation. These data suggest that this bioactive polymer has properties which may be beneficial in the treatment of wound healing.

  11. The Influence of Na and Ti on the In Vitro Degradation and Bioactivity in 58S Sol-Gel Bioactive Glass

    Directory of Open Access Journals (Sweden)

    Shirong Ni

    2012-01-01

    Full Text Available The aim of this study was to investigate the effect of Na and Ti on the in vitro degradation and bioactivity in the 58S bioactive glass. The degradation was evaluated through the activation energy of Si ion release from bioactive glasses and the weight loss of bioactive glasses in Tris-HCl buffer solution. The in vitro bioactivity of the bioactive glasses was investigated by analysis of apatite-formation ability in the simulated body fluid (SBF. The results showed that Na in the 58S glass accelerated the dissolution rate of the glass, whereas Ti in the 58S glass slowed down the rate of glass solubility. Bioactivity tests showed that Na in glass increased the apatite-forming ability in SBF. In contrast, Ti in glass retards the apatite formation at the initial stage of SBF soaking but does not affect the growth of apatite after long periods of soaking.

  12. Megalanthine, a bioactive sesquiterpenoid from Heliotropium megalanthum, its degradation products and their bioactivities.

    Science.gov (United States)

    Macías, Francisco A; Simonet, Ana M; D'Abrosca, Brigida; Maya, Claudia C; Reina, Matías; González-Coloma, Azucena; Cabrera, Raimundo; Giménez, Cristina; Villarroel, Luis

    2009-01-01

    The new bioactive sesquiterpenoid (3R,6E)-2,6,10-trimethyl-3-(3-p-hydroxyphenylpropanoyloxy)-dodeca-6,11-diene-2,10-diol, named megalanthine, was isolated from the resinous exudates of Heliotropium megalanthum. The degradation products of this compound were identified. Several plant-defensive properties (insecticidal, antifungal, and phytotoxic) were evaluated after obtaining positive results in a preliminary etiolated wheat coleoptile bioassay. This bioassay showed the need to have both the phenolic and sesquiterpene moieties of the natural product present to achieve a biological effect. This result was confirmed in phytotoxicity bioassays. Megalanthine was ruled out as a significant plant-plant defense agent because of its lack of stability. The positive results recorded in the antifungal and antifeedant tests suggest, however, that this chemical is relevant in several ecological interactions involving H. megalanthum.

  13. Silicon Utilizing Microbial Bioactivities in the Biosphere

    Science.gov (United States)

    Sen, M. M.; Das, S.

    2012-12-01

    potential as a source of biomass for the production of biofuels, due to their high growth rates and high cellular lipid content. Petroleum pollutant degradation can also be done by these organisms-Achanthes minutissima has degradable effects involving petroleum hydocarbons. Stephanopyxis turris a silicon utilizing organism releases a blend of chlorinated C8 hydrocarbons. This adds a fundamentally new pathway to the limited set of halogenating enzymatic activities known from nature. Many silicon utilizing organisms can produce PUFA from saturated fatty acids which ultimately produce many important bioactive chemicals like hormosirene, finaverrene, heptadienal, dietyopterene, cystophorene, decadienal. Trienoic acid, octadiene and many other important agents. Similarly terpenoid biosynthetic pathway is activated by them with formation of diterpenoids, sesterpenoids, triterpenoids and sterols.

  14. Anti-Inflammatory and Immunoregulatory Functions of Artemisinin and Its Derivatives

    Directory of Open Access Journals (Sweden)

    Chenchen Shi

    2015-01-01

    Full Text Available Artemisinin and its derivatives are widely used in the world as the first-line antimalarial drug. Recently, growing evidences reveal that artemisinin and its derivatives also possess potent anti-inflammatory and immunoregulatory properties. Meanwhile, researchers around the world are still exploring the unknown bioactivities of artemisinin derivatives. In this review, we provide a comprehensive discussion on recent advances of artemisinin derivatives affecting inflammation and autoimmunity, the underlying molecular mechanisms, and also drug development of artemisinins beyond antimalarial functions.

  15. Bioactivity of calcium phosphate bioceramic coating fabricated by laser cladding

    Science.gov (United States)

    Zhu, Yizhi; Liu, Qibin; Xu, Peng; Li, Long; Jiang, Haibing; Bai, Yang

    2016-05-01

    There were always strong expectations for suitable biomaterials used for bone regeneration. In this study, to improve the biocompatiblity of titanium alloy, calcium phosphate bioceramic coating was obtained by laser cladding technology. The microstructure, phases, bioactivity, cell differentiation, morphology and resorption lacunae were investigated by optical microscope (OM), x-ray diffraction (XRD), methyl thiazolyl tetrazolium (MTT) assay, tartrate-resistant acid phosphatase (TRAP) staining and scanning electronic microscope (SEM), respectively. The results show that bioceramic coating consists of three layers, which are a substrate, an alloyed layer and a ceramic layer. Bioactive phases of β-tricalcium phosphate (β-TCP) and hydroxyapatite (HA) were found in ceramic coating. Osteoclast precursors have excellent proliferation on the bioceramic surface. The bioceramics coating could be digested by osteoclasts, which led to the resorption lacunae formed on its surface. It revealed that the gradient bioceramic coating has an excellent bioactivity.

  16. Bioactivity of calcium phosphate bioceramic coating fabricated by laser cladding

    International Nuclear Information System (INIS)

    Zhu, Yizhi; Liu, Qibin; Xu, Peng; Li, Long; Jiang, Haibing; Bai, Yang

    2016-01-01

    There were always strong expectations for suitable biomaterials used for bone regeneration. In this study, to improve the biocompatiblity of titanium alloy, calcium phosphate bioceramic coating was obtained by laser cladding technology. The microstructure, phases, bioactivity, cell differentiation, morphology and resorption lacunae were investigated by optical microscope (OM), x-ray diffraction (XRD), methyl thiazolyl tetrazolium (MTT) assay, tartrate-resistant acid phosphatase (TRAP) staining and scanning electronic microscope (SEM), respectively. The results show that bioceramic coating consists of three layers, which are a substrate, an alloyed layer and a ceramic layer. Bioactive phases of β-tricalcium phosphate (β-TCP) and hydroxyapatite (HA) were found in ceramic coating. Osteoclast precursors have excellent proliferation on the bioceramic surface. The bioceramics coating could be digested by osteoclasts, which led to the resorption lacunae formed on its surface. It revealed that the gradient bioceramic coating has an excellent bioactivity. (letter)

  17. Bioactive Compounds and Antioxidant Activity in Different Types of Berries

    Directory of Open Access Journals (Sweden)

    Sona Skrovankova

    2015-10-01

    Full Text Available Berries, especially members of several families, such as Rosaceae (strawberry, raspberry, blackberry, and Ericaceae (blueberry, cranberry, belong to the best dietary sources of bioactive compounds (BAC. They have delicious taste and flavor, have economic importance, and because of the antioxidant properties of BAC, they are of great interest also for nutritionists and food technologists due to the opportunity to use BAC as functional foods ingredients. The bioactive compounds in berries contain mainly phenolic compounds (phenolic acids, flavonoids, such as anthocyanins and flavonols, and tannins and ascorbic acid. These compounds, either individually or combined, are responsible for various health benefits of berries, such as prevention of inflammation disorders, cardiovascular diseases, or protective effects to lower the risk of various cancers. In this review bioactive compounds of commonly consumed berries are described, as well as the factors influencing their antioxidant capacity and their health benefits.

  18. In vitro bioactivity of glass-ceramic/fibroin composites

    Directory of Open Access Journals (Sweden)

    Lachezar Radev

    2017-06-01

    Full Text Available Bioactive composite materials were prepared by mixing 20 wt.% of silk fibroin (SF and 80 wt.% of glassceramics from CaO-SiO2-P2O5-MgO system. In vitro bioactivity of the prepared composites was evaluated in 1.5 simulated body fluid (1.5 SBF in static conditions. The obtained samples before and after in vitro tests were characterized by X-ray diffraction (XRD analysis, Fourier transform infrared spectroscopy (FTIR, and X-ray photoelectron spectroscopy (XPS. The changes in 1.5 SBF solutions after soaking the samples were evaluated by inductively coupled plasma atomic emission spectroscopy (ICP-AES. MG63 osteosarcoma cells were used for the biological experiments. The obtained experimental data proved that the synthesized composites exhibit excellent in vitro bioactivity.

  19. Bioactive secondary metabolites from marine microbes for drug discovery.

    Science.gov (United States)

    Nikapitiya, Chamilani

    2012-01-01

    The isolation and extraction of novel bioactive secondary metabolites from marine microorganisms have a biomedical potential for future drug discovery as the oceans cover 70% of the planet's surface and life on earth originates from sea. Wide range of novel bioactive secondary metabolites exhibiting pharmacodynamic properties has been isolated from marine microorganisms and many to be discovered. The compounds isolated from marine organisms (macro and micro) are important in their natural form and also as templates for synthetic modifications for the treatments for variety of deadly to minor diseases. Many technical issues are yet to overcome before wide-scale bioprospecting of marine microorganisms becomes a reality. This chapter focuses on some novel secondary metabolites having antitumor, antivirus, enzyme inhibitor, and other bioactive properties identified and isolated from marine microorganisms including bacteria, actinomycetes, fungi, and cyanobacteria, which could serve as potentials for drug discovery after their clinical trials. Copyright © 2012 Elsevier Inc. All rights reserved.

  20. Bioactive glass 45S5 from diatom biosilica

    Directory of Open Access Journals (Sweden)

    Luqman A. Adams

    2017-12-01

    Full Text Available A major draw-back to large scale production of bioactive glasses is the high cost of the standard silica precursor, usually tetraethyl orthosilicate (TEOS. The current study describes a novel sol–gel preparation of 45S5 bioactive glass using diatom biosilica from cultured cells of the diatom, Aulacoseira granulata as substitute to TEOS. The glass formed was characterized using mechanical tester, scanning electron microscopy (SEM, energy dispersive X-ray analysis (EDX, X-ray diffraction (XRD and Fourier transform infrared (FTIR spectroscopy. Results showed that the glass possessed a compressive strength of 3.75 ± 0.18 and formed carbonated hydroxyapatite (HCA within 7 days in simulated body fluid (SBF, attributable to good surface chemistry. The performance of the glass was compared with that of those formed using TEOS. Diatom biosilica could be a potential economically friendly starting material for large scale fabrication of bioactive glasses.

  1. Potential of Fruit Wastes as Natural Resources of Bioactive Compounds

    Directory of Open Access Journals (Sweden)

    Wen-Hua Ling

    2012-07-01

    Full Text Available Fruit wastes are one of the main sources of municipal waste. In order to explore the potential of fruit wastes as natural resources of bioactive compounds, the antioxidant potency and total phenolic contents (TPC of lipophilic and hydrophilic components in wastes (peel and seed of 50 fruits were systematically evaluated. The results showed that different fruit residues had diverse antioxidant potency and the variation was very large. Furthermore, the main bioactive compounds were identified and quantified, and catechin, cyanidin 3-glucoside, epicatechin, galangin, gallic acid, homogentisic acid, kaempferol, and chlorogenic acid were widely found in these residues. Especially, the values of ferric-reducing antioxidant power (FRAP, trolox equivalent antioxidant capacity (TEAC and TPC in the residues were higher than in pulps. The results showed that fruit residues could be inexpensive and readily available resources of bioactive compounds for use in the food and pharmaceutical industries.

  2. SpirPep: an in silico digestion-based platform to assist bioactive peptides discovery from a genome-wide database.

    Science.gov (United States)

    Anekthanakul, Krittima; Hongsthong, Apiradee; Senachak, Jittisak; Ruengjitchatchawalya, Marasri

    2018-04-20

    Bioactive peptides, including biological sources-derived peptides with different biological activities, are protein fragments that influence the functions or conditions of organisms, in particular humans and animals. Conventional methods of identifying bioactive peptides are time-consuming and costly. To quicken the processes, several bioinformatics tools are recently used to facilitate screening of the potential peptides prior their activity assessment in vitro and/or in vivo. In this study, we developed an efficient computational method, SpirPep, which offers many advantages over the currently available tools. The SpirPep web application tool is a one-stop analysis and visualization facility to assist bioactive peptide discovery. The tool is equipped with 15 customized enzymes and 1-3 miscleavage options, which allows in silico digestion of protein sequences encoded by protein-coding genes from single, multiple, or genome-wide scaling, and then directly classifies the peptides by bioactivity using an in-house database that contains bioactive peptides collected from 13 public databases. With this tool, the resulting peptides are categorized by each selected enzyme, and shown in a tabular format where the peptide sequences can be tracked back to their original proteins. The developed tool and webpages are coded in PHP and HTML with CSS/JavaScript. Moreover, the tool allows protein-peptide alignment visualization by Generic Genome Browser (GBrowse) to display the region and details of the proteins and peptides within each parameter, while considering digestion design for the desirable bioactivity. SpirPep is efficient; it takes less than 20 min to digest 3000 proteins (751,860 amino acids) with 15 enzymes and three miscleavages for each enzyme, and only a few seconds for single enzyme digestion. Obviously, the tool identified more bioactive peptides than that of the benchmarked tool; an example of validated pentapeptide (FLPIL) from LC-MS/MS was demonstrated. The

  3. Quantum-chemical study on the bioactive conformation of epothilones.

    Science.gov (United States)

    Jiménez, Verónica A

    2010-12-27

    Herein, I report a DFT study on the bioactive conformation of epothilone A based on the analysis of 92 stable conformations of free and bound epothilone to a reduced model of tubulin receptor. The equilibrium structures and relative energies were studied using B3LYP and X3LYP functionals and the 6-31G(d) standard basis set, which was considered appropriate for the size of the systems under study. Calculated relative energies of free and bound epothilones led me to propose a new model for the bioactive conformation of epothilone A, which accounts for several structure-activity data.

  4. Enhanced Bioactivity of α-Tocopheryl Succinate Based Block Copolymer Nanoparticles by Reduced Hydrophobicity.

    Science.gov (United States)

    Palao-Suay, Raquel; Aguilar, María Rosa; Parra-Ruiz, Francisco J; Maji, Samarendra; Hoogenboom, Richard; Rohner, Nathan A; Thomas, Susan N; Román, Julio San

    2016-12-01

    Well-structured amphiphilic copolymers are necessary to obtain self-assembled nanoparticles (NPs) based on synthetic polymers. Highly homogeneous and monodispersed macromolecules obtained by controlled polymerization have successfully been used for this purpose. However, disaggregation of the organized macromolecules is desired when a bioactive element, such as α-tocopheryl succinate, is introduced in self-assembled NPs and this element must be exposed or released to exert its action. The aim of this work is to demonstrate that the bioactivity of synthetic NPs based on defined reversible addition-fragmentation chain transfer polymerization copolymers can be enhanced by the introduction of hydrophilic comonomers in the hydrophobic segment. The amphiphilic terpolymers are based on poly(ethylene glycol) (PEG) as hydrophilic block, and a hydrophobic block based on a methacrylic derivative of α-tocopheryl succinate (MTOS) and small amounts of 2-hydroxyethyl methacrylate (HEMA) (PEG-b-poly(MTOS-co-HEMA)). The introduction of HEMA reduces hydrophobicity and introduces "disorder" both in the homogeneous blocks and the compact core of the corresponding NPs. These NPs are able to encapsulate additional α-tocopheryl succinate (α-TOS) with high efficiency and their biological activity is much higher than that described for the unmodified copolymers, proposedly due to more efficient degradation and release of α-TOS, demonstrating the importance of the hydrophilic-hydrophobic balance. © 2016 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

  5. Bioactivity of different enriched phenolic extracts of wild fruits from Northeastern Portugal: a comparative study.

    Science.gov (United States)

    Guimarães, Rafaela; Barros, Lillian; Calhelha, Ricardo C; Carvalho, Ana Maria; Queiroz, Maria João R P; Ferreira, Isabel C F R

    2014-03-01

    Arbutus unedo, Prunus spinosa, Rosa micrantha and Rosa canina are good sources of phenolic compounds, including anthocyanins. These compounds have potent antioxidant properties, which have been related to anticancer activity. Herein, the in vitro antioxidant and antitumor properties of enriched phenolic extracts (non-anthocyanin phenolic compounds enriched extract- PE and anthocyanins enriched extract- AE) of the mentioned wild fruits were evaluated and compared. PE gave higher bioactive properties than the corresponding AE. It was observed a high capacity of A. unedo phenolic extract to inhibit lipid peroxidation in animal brain homogenates (EC50 = 7.21 μg/mL), as also a high antitumor potential against NCI-H460 human cell line (non-small lung cancer; GI50 = 37.68 μg/mL), which could be related to the presence of galloyl derivatives (exclusively found in this species). The bioactivity of the studied wild fruits proved to be more related to the phenolic compounds profile than to the amounts present in each extract, and could be considered in the design of new formulations of dietary supplements or functional foods.

  6. Characterization and bioactivity of nano-submicro octacalcium phosphate/gelatin composite

    International Nuclear Information System (INIS)

    Miura, Kei-ichiro; Anada, Takahisa; Honda, Yoshitomo; Shiwaku, Yukari; Kawai, Tadashi; Echigo, Seishi; Takahashi, Tetsu; Suzuki, Osamu

    2013-01-01

    The present study was designed to investigate the physicochemical and bioactive properties of a nano-submicro sized octacalcium phosphate (OCP)-dispersed gelatin (Gel) composite (nano-submicro OCP/Gel) used as a bone substitute material in various bone defects. Well-grown, synthesized OCP was mechanically ground from 100 to 300 μm-sieved granules to particles that were approximately 500 nm in size. Then, 50 wt% of the nano-submicro OCP was mixed with porcine skin-derived acid extracted gelatin. The mixture was molded and lyophilized and then subjected to dehydrothermal crosslinking. X-ray diffraction (XRD) and Fourier transform infrared (FTIR) spectroscopy showed that the structure of OCP was retained even after mechanical grinding to a nano-submicro scale level as well as inclusion in the Gel matrix. The bioactivity of nano-submicro OCP/Gel was examined by immersing the composite in simulated body fluid (SBF) for 7 days and by implanting it in rat critical-sized calvaria defects for 8 weeks. The nano-submicro OCP tended to convert to low crystalline hydroxyapatite (HA) in SBF as assessed by XRD. The nano-submicro OCP/Gel exhibited osteoconductivity in vivo, yielding new bone formation that was closely associated with the implanted composite. These results suggest that the nano-submicro OCP/Gel composite exhibits similar osteoconductivity as observed in other OCP-based materials previously reported and could be used as a bone substitute material for repairing various defects in bone.

  7. Truncation studies of alpha-melanotropin peptides identify tripeptide analogues exhibiting prolonged agonist bioactivity.

    Science.gov (United States)

    Haskell-Luevano, C; Sawyer, T K; Hendrata, S; North, C; Panahinia, L; Stum, M; Staples, D J; Castrucci, A M; Hadley, M F; Hruby, V J

    1996-01-01

    Truncation studies of alpha-melanotropin peptides identify tripeptide analogues exhibiting prolonged agonist bioactivity: PEPTIDES 17(6) 995-1002, 1996.-Systematic analysis of fragment derivatives of the superpotent alpha-MSH analogue. Ac-Ser.Tyr-Ser-Nle4-Glu- His-DPhe7-Arg-Trp-Gly-Lys-Pro-Val-NH2(NDP-MSH), led to the discovery of tripeptide agonists possessing prolonged bioactivity in the frog skin assay. Of particular significance to this discovery was Ac-DPhe-Arg-DTrp-NH2, which was the most potent tripeptide in this series exhibiting sustained melanotropic activity. Different pharmacophore models appear to exist that are dependent on the substructure and stereochemistry of the MSH(6-9) "active site." The tripeptides Ac-DPhe-Arg-Trp-NH2, Ac-DPhe-Arg-DTrp-NH2, and Ac-DPhe-DArg-Trp-NH2 stereo-chemical combinations require only Phe7-Xaa8-Trp9, whereas Ac-DPhe-DArg-DTrp-NH2, Ac-Phe-Arg-DTrp-NH2, and Ac-Phe-Arg-Trp-NH2 additionally require His4 for minimal biological activity. Ac-DPhe-Arg-DTrp-NH2 represents a novel prototype lead for the development of MSH-based peptidomimetic agonists.

  8. Bioactive Wollastonite-Diopside Foams from Preceramic Polymers and Reactive Oxide Fillers

    Directory of Open Access Journals (Sweden)

    Laura Fiocco

    2015-05-01

    Full Text Available Wollastonite (CaSiO3 and diopside (CaMgSi2O6 silicate ceramics have been widely investigated as highly bioactive materials, suitable for bone tissue engineering applications. In the present paper, highly porous glass-ceramic foams, with both wollastonite and diopside as crystal phases, were developed from the thermal treatment of silicone polymers filled with CaO and MgO precursors, in the form of micro-sized particles. The foaming was due to water release, at low temperature, in the polymeric matrix before ceramic conversion, mainly operated by hydrated sodium phosphate, used as a secondary filler. This additive proved to be “multifunctional”, since it additionally favored the phase development, by the formation of a liquid phase upon firing, in turn promoting the ionic interdiffusion. The liquid phase was promoted also by the incorporation of powders of a glass crystallizing itself in wollastonite and diopside, with significant improvements in both structural integrity and crushing strength. The biological characterization of polymer-derived wollastonite-diopside foams, to assess the bioactivity of the samples, was performed by means of a cell culture test. The MTT assay and LDH activity tests gave positive results in terms of cell viability.

  9. Facilitated uptake of a bioactive metabolite of maritime pine bark extract (pycnogenol into human erythrocytes.

    Directory of Open Access Journals (Sweden)

    Max Kurlbaum

    Full Text Available Many plant secondary metabolites exhibit some degree of biological activity in humans. It is a common observation that individual plant-derived compounds in vivo are present in the nanomolar concentration range at which they usually fail to display measurable activity in vitro. While it is debatable that compounds detected in plasma are not the key effectors of bioactivity, an alternative hypothesis may take into consideration that measurable concentrations also reside in compartments other than plasma. We analysed the binding of constituents and the metabolite δ-(3,4-dihydroxy-phenyl-γ-valerolactone (M1, that had been previously detected in plasma samples of human consumers of pine bark extract Pycnogenol, to human erythrocytes. We found that caffeic acid, taxifolin, and ferulic acid passively bind to red blood cells, but only the bioactive metabolite M1 revealed pronounced accumulation. The partitioning of M1 into erythrocytes was significantly diminished at higher concentrations of M1 and in the presence of glucose, suggesting a facilitated transport of M1 via GLUT-1 transporter. This concept was further supported by structural similarities between the natural substrate α-D-glucose and the S-isomer of M1. After cellular uptake, M1 underwent further metabolism by conjugation with glutathione. We present strong indication for a transporter-mediated accumulation of a flavonoid metabolite in human erythrocytes and subsequent formation of a novel glutathione adduct. The physiologic role of the adduct remains to be elucidated.

  10. The role of ATP-binding cassette transporters in neuro-inflammation: relevance for bioactive lipids

    Directory of Open Access Journals (Sweden)

    Gijs eKooij

    2012-04-01

    Full Text Available ATP-binding cassette (ABC transporters are highly expressed by brain endothelial cells that form the blood-brain barrier (BBB. These efflux pumps play an important role in maintaining brain homeostasis as they actively hinder the entry of unwanted blood-derived compounds into the central nervous system (CNS. Consequently, their high activity at the BBB has been a major hurdle for the treatment of several brain diseases, as they prevent numerous drugs to reach their site of action within the brain. Importantly, recent data indicate that endogenous substrates for ABC transporters may include inflammatory mediators, such as prostaglandins, leukotrienes, cytokines, chemokines and bioactive lipids, suggesting a potential role for ABC transporters in immunological responses, and more specifically in inflammatory brain disorders, such as multiple sclerosis (MS. In this review, we will give a comprehensive overview of recent findings that illustrate this novel role for ABC transporters in neuro-inflammatory processes. Moreover, we will provide first insights into underlying mechanisms and focus on the importance for bioactive lipids, in particular platelet-activating factor (PAF, herein. A thorough understanding of these events may form the basis for the development for selective treatment modalities to dampen the neuro-inflammatory attack in MS and thereby reducing tissue damage.

  11. Empirical modeling of drying kinetics and microwave assisted extraction of bioactive compounds from Adathoda vasica

    Directory of Open Access Journals (Sweden)

    Prithvi Simha

    2016-03-01

    Full Text Available To highlight the shortcomings in conventional methods of extraction, this study investigates the efficacy of Microwave Assisted Extraction (MAE toward bioactive compound recovery from pharmaceutically-significant medicinal plants, Adathoda vasica and Cymbopogon citratus. Initially, the microwave (MW drying behavior of the plant leaves was investigated at different sample loadings, MW power and drying time. Kinetics was analyzed through empirical modeling of drying data against 10 conventional thin-layer drying equations that were further improvised through the incorporation of Arrhenius, exponential and linear-type expressions. 81 semi-empirical Midilli equations were derived and subjected to non-linear regression to arrive at the characteristic drying equations. Bioactive compounds recovery from the leaves was examined under various parameters through a comparative approach that studied MAE against Soxhlet extraction. MAE of A. vasica reported similar yields although drastic reduction in extraction time (210 s as against the average time of 10 h in the Soxhlet apparatus. Extract yield for MAE of C. citratus was higher than the conventional process with optimal parameters determined to be 20 g sample load, 1:20 sample/solvent ratio, extraction time of 150 s and 300 W output power. Scanning Electron Microscopy and Fourier Transform Infrared Spectroscopy were performed to depict changes in internal leaf morphology.

  12. Development of bioactive coatings based on γ-irradiated proteins to preserve strawberries

    International Nuclear Information System (INIS)

    Vu, K.D.; Hollingsworth, R.G.; Salmieri, S.; Takala, P.N.; Lacroix, M.

    2012-01-01

    Gamma irradiation was applied for creating cross-linked proteins to enhance the physicochemical properties of edible films made of calcium caseinate, whey protein isolate and glycerol. The characteristics of γ irradiated cross-linked proteins were analyzed by Fourier Transform Infrared spectroscopy. A second derivative spectra exhibited changes in band intensities that were correlated to an increase of β-sheet structure and a decrease of α-helix and unordered fractions of γ irradiated-cross-linked proteins as compared to the control without irradiation. Furthermore, on addition of methylcellulose to the irradiated protein matrix it was found that it has potential in enhancing the puncture strength and has no detrimental effect on water vapor permeability of protein based films. Finally, these film formulations were used as bioactive edible coatings containing natural antimicrobial agents (limonene and peppermint) to preserve the shelf life of fresh strawberries during storage. The bioactive coatings containing peppermint was found to be more efficient as preserving coatings than the formulations containing limonene. Irradiated proteins/methylcellulose/peppermint formulation had only 40% of decay at day 8 while it was 65% for the control. - Highlights: ► Crosslinked proteins and antimicrobials agents was able to preserve strawberries. ► Crosslinked protein structure was more ordered. ► Films based on crosslinked proteins and methylcellulose enhanced puncture strength.

  13. Characterization and bioactivity of nano-submicro octacalcium phosphate/gelatin composite

    Energy Technology Data Exchange (ETDEWEB)

    Miura, Kei-ichiro [Division of Craniofacial Function Engineering, Tohoku University Graduate School of Dentistry, Sendai (Japan); Division of Oral and Maxillofacial Surgery, Tohoku University Graduate School of Dentistry, Sendai (Japan); Anada, Takahisa; Honda, Yoshitomo [Division of Craniofacial Function Engineering, Tohoku University Graduate School of Dentistry, Sendai (Japan); Shiwaku, Yukari [Division of Craniofacial Function Engineering, Tohoku University Graduate School of Dentistry, Sendai (Japan); Division of Advanced Prosthetic Dentistry, Tohoku University Graduate School of Dentistry, Sendai (Japan); Kawai, Tadashi; Echigo, Seishi; Takahashi, Tetsu [Division of Oral and Maxillofacial Surgery, Tohoku University Graduate School of Dentistry, Sendai (Japan); Suzuki, Osamu, E-mail: suzuki-o@m.tohoku.ac.jp [Division of Craniofacial Function Engineering, Tohoku University Graduate School of Dentistry, Sendai (Japan)

    2013-10-01

    The present study was designed to investigate the physicochemical and bioactive properties of a nano-submicro sized octacalcium phosphate (OCP)-dispersed gelatin (Gel) composite (nano-submicro OCP/Gel) used as a bone substitute material in various bone defects. Well-grown, synthesized OCP was mechanically ground from 100 to 300 μm-sieved granules to particles that were approximately 500 nm in size. Then, 50 wt% of the nano-submicro OCP was mixed with porcine skin-derived acid extracted gelatin. The mixture was molded and lyophilized and then subjected to dehydrothermal crosslinking. X-ray diffraction (XRD) and Fourier transform infrared (FTIR) spectroscopy showed that the structure of OCP was retained even after mechanical grinding to a nano-submicro scale level as well as inclusion in the Gel matrix. The bioactivity of nano-submicro OCP/Gel was examined by immersing the composite in simulated body fluid (SBF) for 7 days and by implanting it in rat critical-sized calvaria defects for 8 weeks. The nano-submicro OCP tended to convert to low crystalline hydroxyapatite (HA) in SBF as assessed by XRD. The nano-submicro OCP/Gel exhibited osteoconductivity in vivo, yielding new bone formation that was closely associated with the implanted composite. These results suggest that the nano-submicro OCP/Gel composite exhibits similar osteoconductivity as observed in other OCP-based materials previously reported and could be used as a bone substitute material for repairing various defects in bone.

  14. New Therapeutic Drugs from Bioactive Natural Molecules: the Role of Gut Microbiota Metabolism in Neurodegenerative Diseases.

    Science.gov (United States)

    Di Meo, Francesco; Donato, Stella; Di Pardo, Alba; Maglione, Vittorio; Filosa, Stefania; Crispi, Stefania

    2018-04-03

    The gut-brain axis is considered a neuroendocrine system, which connects brain and gastrointestinal tract and plays an important role in stress response. The homeostasis of gut-brain axis is important for healthy conditions and its alterations are associated to neurological disorders and neurodegenerative diseases. Gut microbiota is a dynamic ecosystem that can be altered by external factors such as diet composition, antibiotics or xenobiotics. Recent advances in gut microbiota analyses indicate that the gut bacterial community plays a key role in maintaining normal brain functions. Recent metagenomic analyses have elucidated that the relationship between gut and brain, either in normal or in pathological conditions, reflects the existence of a "microbiota-gut-brain" axis. Gut microbiota composition can be influenced by dietary ingestion of probiotics or natural bioactive molecules such as prebiotics and polyphenols. Their derivatives coming from microbiota metabolism can affect both gut bacterial composition and brain biochemistry. Modifications of microbiota composition by natural bioactive molecules could be used to restore the altered brain functions, which characterize neurodegenerative diseases, leading to consider these compounds as novel therapeutic strategies for the treatment of neuropathologies. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

  15. Bioactivity-guided isolation of laevicarpin, an antitrypanosomal and anticryptococcal lactam from Piper laevicarpu (Piperaceae).

    Science.gov (United States)

    da Silva A Maciel, Dayany; Freitas, Viviane P; Conserva, Geanne A Alves; Alexandre, Tatiana R; Purisco, Sonia U; Tempone, Andre G; Melhem, Márcia Souza C; Kato, Massuo J; Guimarães, Elsie F; Lago, João Henrique G

    2016-06-01

    Crude CH2Cl2 extract from leaves of Piper laevicarpu (Piperaceae) displayed antitrypanosomal activity against trypomastigote forms of Trypanosoma cruzi (Y strain) and antimicrobial potential against Cryptococcus gattii (strain-type WM 178). Bioactivity-guided fractionation of crude extract afforded one new natural bioactive lactam derivative, named laevicarpin. The structure of isolated compound, which displayed a very rare ring system, was elucidated based on NMR, IR and MS spectral analysis. Using MTT assay, the trypomastigotes of T. cruzi demonstrated susceptibility to laevicarpin displaying IC50 value of 14.7μg/mL (49.6μM), about 10-fold more potent than the standard drug benznidazole. The mammalian cytotoxicity of laevicarpin was verified against murine fibroblasts (NCTC cells) and demonstrated a CC50 value of 100.3μg/mL (337.7μM-SI=7). When tested against Cryptococcus gattii, laevicarpin showed an IC50 value of 2.3μg/mL (7.9μM) and a MIC value of 7.4μg/mL (25μM). Based in the obtained results, laevicarpin could be used as a scaffold for future drug design studies against the Chagas disease and anti-cryptococosis agents. Copyright © 2016 Elsevier B.V. All rights reserved.

  16. The Role of Bioactive Lipids in Stem Cell Mobilization and Homing: Novel Therapeutics for Myocardial Ischemia

    Directory of Open Access Journals (Sweden)

    Yuri M. Klyachkin

    2014-01-01

    Full Text Available Despite significant advances in medical therapy and interventional strategies, the prognosis of millions of patients with acute myocardial infarction (AMI and ischemic heart disease (IHD remains poor. Currently, short of heart transplantation with all of its inherit limitations, there are no available treatment strategies that replace the infarcted myocardium. It is now well established that cardiomyocytes undergo continuous renewal, with contribution from bone marrow (BM-derived stem/progenitor cells (SPCs. This phenomenon is upregulated during AMI by initiating multiple innate reparatory mechanisms through which BMSPCs are mobilized towards the ischemic myocardium and contribute to myocardial regeneration. While a role for the SDF-1/CXCR4 axis in retention of BMSPCs in bone marrow is undisputed, its exclusive role in their mobilization and homing to a highly proteolytic microenvironment, such as the ischemic/infarcted myocardium, is currently being challenged. Recent evidence suggests a pivotal role for bioactive lipids in the mobilization of BMSPCs at the early stages following AMI and their homing towards ischemic myocardium. This review highlights the recent advances in our understanding of the mechanisms of stem cell mobilization, provides newer evidence implicating bioactive lipids in BMSPC mobilization and differentiation, and discusses their potential as therapeutic agents in the treatment of IHD.

  17. Bioactivity-guided mixed synthesis accelerate the serendipity in lead optimization: Discovery of fungicidal homodrimanyl amides.

    Science.gov (United States)

    Li, Dangdang; Zhang, Shasha; Song, Zehua; Wang, Guotong; Li, Shengkun

    2017-08-18

    The bioactivity-guided mixed synthesis was conceived, in which the designed mix-reactions were run in parallel for simultaneous construction of different kinds of analogs. The valuable ones were protruded by biological screening. This tactic will facilitate more rapid incorporation of bioactive candidates into pesticide chemists' repertoire, exemplified by the optimization of less explored homodrimanes as antifungal ingredients. The discovery of D9 as a potent fungicidal agent can be completed in <2 weeks by one student, with EC 50 of 3.33 mg/L and 2.45 mg/L against S. sclerotiorum and B. cinerea, respectively. To confirm the practicability, time-efficiency, and reliability, specific homodrimanes (82 derivatives) were synthesized and elucidated separately and determined for EC 50 values. The SAR correlated well with the intentionally mixed synthesis and the potential was further confirmed by the in vivo bioassay. This methodology will foster more efficient exploration of biologically relevant chemical space of natural products in pesticide discovery, and can also be tailored readily for the lead optimization in medicinal chemistry. Copyright © 2017 Elsevier Masson SAS. All rights reserved.

  18. State of the Art on Functional Virgin Olive Oils Enriched with Bioactive Compounds and Their Properties

    Directory of Open Access Journals (Sweden)

    Patricia Reboredo-Rodríguez

    2017-03-01

    Full Text Available Virgin olive oil, the main fat of the Mediterranean diet, is per se considered as a functional food—as stated by the European Food Safety Authority (EFSA—due to its content in healthy compounds. The daily intake of endogenous bioactive phenolics from virgin olive oil is variable due to the influence of multiple agronomic and technological factors. Thus, a good strategy to ensure an optimal intake of polyphenols through habitual diet would be to produce enriched virgin olive oil with well-known bioactive polyphenols. Different sources of natural biological active substances can be potentially used to enrich virgin olive oil (e.g., raw materials derived from the same olive tree, mainly olive leaves and pomaces, and/or other compounds from plants and vegetables, mainly herbs and spices. The development of these functional olive oils may help in prevention of chronic diseases (such as cardiovascular diseases, immune frailty, ageing disorders and degenerative diseases and improving the quality of life for many consumers reducing health care costs. In the present review, the most relevant scientific information related to the development of enriched virgin olive oil and their positive human health effects has been collected and discussed.

  19. Rat health status affects bioavailability, target tissue levels, and bioactivity of grape seed flavanols

    NARCIS (Netherlands)

    Margalef, M.; Pons, Z.; Iglesias-Carres, L.; Quinones, M.; Bravo, F.I.; Arola-Arnal, A.; Muguerza, B.

    2017-01-01

    SCOPE: Studying the flavanol metabolism is essential to identify bioactive compounds, as beneficial effects of flavanols have been attributed to their metabolic products. However, host-related factors, including pathological conditions, may affect flavanol metabolism and, thus, their bioactivity.

  20. Nano/macro porous bioactive glass scaffold

    Science.gov (United States)

    Wang, Shaojie

    Bioactive glass (BG) and ceramics have been widely studied and developed as implants to replace hard tissues of the musculo-skeletal system, such as bones and teeth. Recently, instead of using bulk materials, which usually do not degrade rapidly enough and may remain in the human body for a long time, the idea of bioscaffold for tissue regeneration has generated much interest. An ideal bioscaffold is a porous material that would not only provide a three-dimensional structure for the regeneration of natural tissue, but also degrade gradually and, eventually be replaced by the natural tissue completely. Among various material choices the nano-macro dual porous BG appears as the most promising candidate for bioscaffold applications. Here macropores facilitate tissue growth while nanopores control degradation and enhance cell response. The surface area, which controls the degradation of scaffold can also be tuned by changing the nanopore size. However, fabrication of such 3D structure with desirable nano and macro pores has remained challenging. In this dissertation, sol-gel process combined with spinodal decomposition or polymer sponge replication method has been developed to fabricate the nano-macro porous BG scaffolds. Macropores up to 100microm are created by freezing polymer induced spinodal structure through sol-gel transition, while larger macropores (>200um) of predetermined size are obtained by the polymer sponge replication technique. The size of nanopores, which are inherent to the sol-gel method of glass fabrication, has been tailored using several approaches: Before gel point, small nanopores are generated using acid catalyst that leads to weakly-branched polymer-like network. On the other hand, larger nanopores are created with the base-catalyzed gel with highly-branched cluster-like structure. After the gel point, the nanostructure can be further modified by manipulating the sintering temperature and/or the ammonia concentration used in the solvent

  1. Bioactivity of Neem (Azadirachta indica) callus extract

    International Nuclear Information System (INIS)

    Ahmed, I.M.

    2008-04-01

    This study was conducted in order to explore the possibility of utilizing plant tissue culture techniques for production of secondary metabolites from callus culture of Azadirachta indica (Neem) and to investigate the bioactivity of the established callus extract in comparison with the extract from the intact leaves. The presence of secondary metabolites in the extracts was detected by Thin Layer Chromatography (TLC). Both the callus and leaf extracts eluted five fraction of compounds and it were observed that callus extract had a good resolution. various extract concentration (5.10. and 20 mg/ml) were determined for the rate and extent of inhibition kinetics against staphylococcus aureus. Escherichia coli, and candida albicans. Results showed that callus extract of A. indica wiped out all viable cells of C. albicans within 18 hours and the subsequent concentration 5 and 10 mg/ m1 retard the growth after 24 h. A higher concentration of 20 mg/ ml had the same effect on S. aureus after 6 h and the E. coli cells were completely inhibited by the extracts after 24 h. Similar kinetics were showed by leaf extract but in slight rate as compared to the callus extract. In general both extract posses antimicrobial activity with notable efficient rates. For assaying of the inhibitory effect on some phyto pathogens the effect of different concentrations of the callus and leaf extracts on the radial growth of Drechslera rostrata. Fusarium oxysporum and Alterneria alternata were in vitro assessed. Obvious inhibitory effect was observed on the mycelia radial growth of the three treated fungi. The level of inhibition increased with the increase of te extract concentration. The maximum inhibitory effect (84%) was recorded with Drechslera rostrata when inoculated in media contain 20 mg/ ml of callus while the inhibition rate of mycelia growth of the same species reaches 61% when inoculated in a medium contain the same concentration of the neem leaf extract. The subsequent

  2. Mass Spectrometric Characteristics of Prenylated Indole Derivatives from Marine-Derived Penicillium sp. NH-SL.

    Science.gov (United States)

    Ding, Hui; Ding, Wanjing; Ma, Zhongjun

    2017-03-22

    Two prenylated indole alkaloids were isolated from the ethyl acetate extracts of a marine-derived fungus Penicillium sp. NH-SL and one of them exhibited potent cytotoxic activity against mouse hepa 1c1c7 cells. In order to detect other bioactive analogs, we used liquid chromatogram tandem mass spectrometry (LC-MS/MS) to analyze the mass spectrometric characteristics of the isolated compounds as well as the crude extracts. As a result, three other analogs were detected, and their structures were deduced according to the similar fragmentation patterns. This is the first systematic report on the mass spectrometric characteristics of prenylated indole derivatives.

  3. Initial boost release of transforming growth factor-β3 and chondrogenesis by freeze-dried bioactive polymer scaffolds.

    Science.gov (United States)

    Krüger, Jan Philipp; Machens, Isabel; Lahner, Matthias; Endres, Michaela; Kaps, Christian

    2014-12-01

    In cartilage regeneration, bio-activated implants are used in stem and progenitor cell-based microfracture cartilage repair procedures. Our aim was to analyze the chondrogenic potential of freeze-dried resorbable polymer-based polyglycolic acid (PGA) scaffolds bio-activated with transforming growth factor-β3 (TGFB3) on human subchondral mesenchymal progenitor cells known from microfracture. Progenitor cells derived from femur heads were cultured in the presence of freeze-dried TGFB3 in high-density pellet culture and in freeze-dried TGFB3-PGA scaffolds for chondrogenic differentiation. Progenitor cell cultures in PGA scaffolds as well as pellet cultures with and without continuous application of TGFB3 served as controls. Release studies showed that freeze-dried TGFB3-PGA scaffolds facilitate a rapid, initial boost-like release of 71.5% of TGFB3 in the first 10 h. Gene expression analysis and histology showed induction of typical chondrogenic markers like type II collagen and formation of cartilaginous tissue in TGFB3-PGA scaffolds seeded with subchondral progenitor cells and in pellet cultures stimulated with freeze-dried TGFB3. Chondrogenic differentiation in freeze-dried TGFB3-PGA scaffolds was comparable to cultures receiving TGFB3 continuously, while non-stimulated controls did not show chondrogenesis during prolonged culture for 14 days. These results suggest that bio-activated, freeze-dried TGFB3-PGA scaffolds have chondrogenic potential and are a promising tool for stem cell-mediated cartilage regeneration.

  4. Bioactive Films Containing Alginate-Pectin Composite Microbeads with Lactococcus lactis subsp. lactis: Physicochemical Characterization and Antilisterial Activity

    Directory of Open Access Journals (Sweden)

    Mariam Bekhit

    2018-02-01

    Full Text Available Novel bioactive films were developed from the incorporation of Lactococcus lactis into polysaccharide films. Two different biopolymers were tested: cellulose derivative (hydroxylpropylmethylcellulose (HPMC and corn starch. Lactic acid bacteria (LAB free or previously encapsulated in alginate-pectin composite hydrogel microbeads were added directly to the film forming solution and films were obtained by casting. In order to study the impact of the incorporation of the protective culture into the biopolymer matrix, the water vapour permeability, oxygen permeability, optical and mechanical properties of the dry films were evaluated. Furthermore, the antimicrobial effect of bioactive films against Listeria monocytogenes was studied in synthetic medium. Results showed that the addition of LAB or alginate-pectin microbeads modified slightly films optical properties. In comparison with HPMC films, starch matrix proves to be more sensitive to the addition of bacterial cells or beads. Indeed, mechanical resistance of corn starch films was lower but barrier properties were improved, certainly related to the possible establishment of interactions between alginate-pectin beads and starch. HPMC and starch films containing encapsulated bioactive culture showed a complete inhibition of listerial growth during the first five days of storage at 5 °C and a reduction of 5 logs after 12 days.

  5. Bio-Activity and Dereplication-Based Discovery of Ophiobolins and Other Fungal Secondary Metabolites Targeting Leukemia Cells

    Directory of Open Access Journals (Sweden)

    Tanja Thorskov Bladt

    2013-11-01

    Full Text Available The purpose of this study was to identify and characterize fungal natural products (NPs with in vitro bioactivity towards leukemia cells. We based our screening on a combined analytical and bio-guided approach of LC-DAD-HRMS dereplication, explorative solid-phase extraction (E-SPE, and a co-culture platform of CLL and stromal cells. A total of 289 fungal extracts were screened and we tracked the activity to single compounds in seven of the most active extracts. The novel ophiobolin U was isolated together with the known ophiobolins C, H, K as well as 6-epiophiobolins G, K and N from three fungal strains in the Aspergillus section Usti. Ophiobolins A, B, C and K displayed bioactivity towards leukemia cells with induction of apoptosis at nanomolar concentrations. The remaining ophiobolins were mainly inactive or only slightly active at micromolar concentrations. Dereplication of those ophiobolin derivatives possessing different activity in combination with structural analysis allowed a correlation of the chemical structure and conformation with the extent of bioactivity, identifying the hydroxy group at C3 and an aldehyde at C21, as well as the A/B-cis ring structure, as indispensible for the strong activity of the ophiobolins. The known compounds penicillic acid, viridicatumtoxin, calbistrin A, brefeldin A, emestrin A, and neosolaniol monoacetate were identified from the extracts and also found generally cytotoxic.

  6. Peptide-laden mesoporous silica nanoparticles with promoted bioactivity and osteo-differentiation ability for bone tissue engineering.

    Science.gov (United States)

    Luo, Zuyuan; Deng, Yi; Zhang, Ranran; Wang, Mengke; Bai, Yanjie; Zhao, Qiang; Lyu, Yalin; Wei, Jie; Wei, Shicheng

    2015-07-01

    Combination of mesoporous silica materials and bioactive factors is a promising niche-mimetic solution as a hybrid bone substitution for bone tissue engineering. In this work, we have synthesized biocompatible silica-based nanoparticles with abundant mesoporous structure, and incorporated bone-forming peptide (BFP) derived from bone morphogenetic protein-7 (BMP-7) into the mesoporous silica nanoparticles (MSNs) to obtain a slow-release system for osteogenic factor delivery. The chemical characterization demonstrates that the small osteogenic peptide is encapsulated in the mesoporous successfully, and the nitrogen adsorption-desorption isotherms suggest that the peptide encapsulation has no influence on mesoporous structure of MSNs. In the cell experiment, the peptide-laden MSNs (p-MSNs) show higher MG-63 cell proliferation, spreading and alkaline phosphatase (ALP) activity than the bare MSNs, indicating good in vitro cytocompatibility. Simultaneously, the osteogenesis-related proteins expression and calcium mineral deposition disclose enhanced osteo-differentiation of human mesenchymal stem cells (hMSCs) under the stimulation of the p-MSNs, confirming that BFP released from MSNs could significantly promote the osteogenic differentiation of hMSCs, especially at 500μg/mL of p-MSNs concentration. The peptide-modified MSNs with better bioactivity and osteogenic differentiation make it a potential candidate as bioactive material for bone repairing, bone regeneration, and bio-implant coating applications. Copyright © 2015 Elsevier B.V. All rights reserved.

  7. Glycation and transglutaminase mediated glycosylation of fish gelatin peptides with glucosamine enhance bioactivity.

    Science.gov (United States)

    Hong, Pui Khoon; Gottardi, Davide; Ndagijimana, Maurice; Betti, Mirko

    2014-01-01

    A mixture of novel glycopeptides from glycosylation between cold water fish skin gelatin hydrolysates and glucosamine (GlcN) via transglutaminase (TGase), as well as glycation between fish gelatin hydrolysate and GlcN were identified by their pattern of molecular distribution using MALDI-TOF-MS. Glycated/glycosylated hydrolysates showed superior bioactivity to their original hydrolysates. Alcalase-derived fish skin gelatin hydrolysate glycosylated with GlcN in the presence of TGase at 25°C (FAT25) possessed antioxidant activity when tested in a linoleic acid oxidation system, when measured according to its 2,2-diphenyl-1-picrylhydrazyl (DPPH) scavenging activity and when tested at the cellular level with human hepatocarcinoma (HepG2) cells as target cells. In addition, Alcalase-derived glycosylated hydrolysates showed specificity toward the inhibition of Escherichia coli (E. coli). The Flavourzyme-derived glycopeptides prepared at 37°C (FFC37 and FFT37) showed better DPPH scavenging activity than their native hydrolysates. The glycated Flavourzyme-derived hydrolysates were found to act as potential antimicrobial agents when incubated with E. coli and Bacillus subtilis. Copyright © 2013 Elsevier Ltd. All rights reserved.

  8. Bioactive components of Gynura divaricata and its potential use in ...

    African Journals Online (AJOL)

    Bioactive components of Gynura divaricata and its potential use in health, food and medicine:a mini-review. Bing-Qing Xu, Yu-Qing Zhang. Abstract. Background: G. divaricata (L.) DC belongs to genus the Gynura Cass which is a kind of perennial herb that has good health protection efficacy and is especially used widely in ...

  9. A novel graded bioactive high adhesion implant coating

    International Nuclear Information System (INIS)

    Brohede, Ulrika; Zhao, Shuxi; Lindberg, Fredrik; Mihranyan, Albert; Forsgren, Johan; Stromme, Maria; Engqvist, Hakan

    2009-01-01

    One method to increase the clinical success rate of metal implants is to increase their bone bonding properties, i.e. to develop a bone bioactive surface leading to reduced risks of interfacial problems. Much research has been devoted to modifying the surface of metals to make them become bioactive. Many of the proposed methods include depositing a coating on the implant. However, there is a risk of coating failure due to low substrate adhesion. This paper describes a method to obtain bioactivity combined with a high coating adhesion via a gradient structure of the coating. Gradient coatings were deposited on Ti (grade 5) using reactive magnetron sputtering with increasing oxygen content. To increase the grain size in the coating, all coatings were post annealed at 385 deg. C. The obtained coating exhibited a gradual transition over 70 nm from crystalline titanium oxide (anatase) at the surface to metallic Ti in the substrate, as shown using cross-section transmission electron microscopy and X-ray photoelectron spectroscopy depth profiling. Using scratch testing, it could be shown that the adhesion to the substrate was well above 1 GPa. The bioactivity of the coating was verified in vitro by the spontaneous formation of hydroxylapatite upon storage in phosphate buffer solution at 37 deg. C for one week. The described process can be applied to implants irrespective of bulk metal in the base and should introduce the possibility to create safer permanent implants like reconstructive devices, dental, or spinal implants.

  10. Antibacterial polylactic acid/chitosan nanofibers decorated with bioactive glass

    Energy Technology Data Exchange (ETDEWEB)

    Goh, Yi-fan; Akram, Muhammad; Alshemary, Ammarz [Department of Chemistry, Faculty of Science, Universiti Teknologi Malaysia, 81310 Johor Bahru, Johor (Malaysia); Hussain, Rafaqat, E-mail: rafaqat@comsats.edu.pk [Department of Physics, COMSATS Institute of Information Technology, Islamabad (Pakistan)

    2016-11-30

    Highlights: • PLA/Chitosan nanofibers were coated with functional bioglass. • Polymer/ceramic composite fibers exhibited good in-vitro bioactivity. • Nanofibers coated with Ag doped bioglass exhibited good antibacterial activity. - Abstract: In this study, we have presented the structural and in vitro characterization of electrospun polylactic acid (PLA)/Chitosan nanofibers coated with cerium, copper or silver doped bioactive glasses (CeBG/CuBG/AgBG). Bead-free, smooth surfaced nanofibers were successfully prepared by using electrospinning technique. The nanocomposite fibers were obtained using a facile dip-coating method, their antibacterial activities against E. coliE. coli (ATCC 25922 strains) were measured by the disk diffusion method after 24 h of incubation at 37 °C. CeBG and CuBG decorated PLA/Chitosan nanofibers did not develop an inhibition zone against the bacteria. On the other hand, nanofibers coated with AgBG developed an inhibition zone against the bacteria. The as-prepared nanocomposite fibers were immersed in SBF for 1, 3 and 7 days in Simulated Body Fluid (SBF) for evaluation of in vitro bioactivity. All samples induced the formation of crystallites with roughly ruffled morphology and the pores of fibers were covered with the extensive growth of crystallites. Energy Dispersive X-ray (EDX) composition analysis showed that the crystallites possessed Ca/P ratio close to 1.67, confirming the good in-vitro bioactivity of the fibers.

  11. Fatty Acid Profile and Bioactivity from Annona hypoglauca Seeds Oil ...

    African Journals Online (AJOL)

    Plants from Annona (Annonaceae) genus are present in tropical regions, where they have economic and medicinal potential. Information on the fatty acids profile and bioactivity from seed oil of Annona species are incipient. The objective of this work was to investigate Annona hypoglauca seeds oil in terms of its yield, ...

  12. Bioactivity-guided mapping and navigation of chemical space

    NARCIS (Netherlands)

    Renner, S.; Otterlo, van W.A.L.; Seoane, M.D.; Möcklinghoff, S.; Hofmann, B.; Wetzel, S.; Schuffenhauer, A.; Ertl, P.; Oprea, T.I.; Steinhilber, D.; Brunsveld, L.; Rauh, D.; Waldmann, H.

    2009-01-01

    The structure- and chemistry-based hierarchical organization of library scaffolds in tree-like arrangements provides a valid, intuitive means to map and navigate chemical space. We demonstrate that scaffold trees built using bioactivity as the key selection criterion for structural simplification

  13. Screening and identification of potential bioactive constituents in a ...

    African Journals Online (AJOL)

    ... of lung cancer, liver cancer and digestive cancer. Materials and Methods: In this study, the potential bioactive constituents of SCP were isolated and identified by chromatographic and spectroscopic methods. The immunomodulatory and DPPH radical scavenging activities of the constituents were also evaluated in vitro.

  14. Advancement into the Arctic Region for Bioactive Sponge Secondary Metabolites

    Science.gov (United States)

    Abbas, Samuel; Kelly, Michelle; Bowling, John; Sims, James; Waters, Amanda; Hamann, Mark

    2011-01-01

    Porifera have long been a reservoir for the discovery of bioactive compounds and drug discovery. Most research in the area has focused on sponges from tropical and temperate waters, but more recently the focus has shifted to the less accessible colder waters of the Antarctic and, to a lesser extent, the Arctic. The Antarctic region in particular has been a more popular location for natural products discovery and has provided promising candidates for drug development. This article reviews groups of bioactive compounds that have been isolated and reported from the southern reaches of the Arctic Circle, surveys the known sponge diversity present in the Arctic waters, and details a recent sponge collection by our group in the Aleutian Islands, Alaska. The collection has yielded previously undescribed sponge species along with primary activity against opportunistic infectious diseases, malaria, and HCV. The discovery of new sponge species and bioactive crude extracts gives optimism for the isolation of new bioactive compounds from a relatively unexplored source. PMID:22163194

  15. Antagonistic bioactivity of an endophytic bacterium isolated from ...

    African Journals Online (AJOL)

    Antagonistic bioactivity of an endophytic bacterium isolated from Epimedium brevicornu Maxim. R He, G Wang, X Liu, C Zhang, F Lin. Abstract. Endophytic bacteria are one of the most potential biological control agents in plant disease protection. The aim of this work was to evaluate the antimicrobial activities of a strain of ...

  16. Effects of bioactive principles from stem bark extract of Quassia ...

    African Journals Online (AJOL)

    Chigo Okwuosa

    Effects of bioactive principles from stem bark extract of Quassia amara, Quassin and 2-methoxycanthine-6-one, on haematological parameters in albino rats. Raji Yinusa. Department of Physiology, College of Medicine, University of Ibadan. Nigeria. Summary:The effect of Quassia amara extract and two isolated compounds ...

  17. Microbial production of astilbin, a bioactive rhamnosylated flavanonol, from taxifolin

    DEFF Research Database (Denmark)

    Thuan, Nguyen Huy; Malla, Sailesh; Trung, Nguyen Thanh

    2017-01-01

    Flavonoids are plant-based polyphenolic biomolecules with a wide range of biological activities. Glycosylated flavonoids have drawn special attention in the industries as it improves solubility, stability, and bioactivity. Herein, we report the production of astilbin (ATN) from taxifolin (TFN) in...

  18. Accelerated bone ingrowth by local delivery of Zinc from bioactive ...

    African Journals Online (AJOL)

    Background: Synthetic bone graft substitutes such as bioactive glass (BG) material are developed in order to achieve successful bone regeneration. Zn plays an important role in the proper bone growth, development, and maintenance of healthy bones. Aims: This study aims to evaluate in vivo the performance therapy of ...

  19. Chitosan/bioactive glass nanoparticle composite membranes for periodontal regeneration

    NARCIS (Netherlands)

    Mota, J.; Yu, N.; Caridade, S.G.; Luz, G.M.; Gomes, M.E.R.; Reis, R.L.; Jansen, J.A.; Walboomers, X.F.; Mano, J.F.

    2012-01-01

    Barrier membranes are used in periodontal applications with the aim of supporting periodontal regeneration by physically blocking migration of epithelial cells. The present work proposes a combination of chitosan (CHT) with bioactive glass nanoparticles (BG-NPs) in order to produce a novel guided

  20. Greener and Expeditious Synthesis of Bioactive Heterocycles using Microwave Irradiation

    Science.gov (United States)

    The utilization of green chemistry techniques is dramatically reducing chemical waste and reaction times as has recently been proven in several organic syntheses and chemical transformations. To illustrate these advantages in the synthesis of bio-active heterocycles, we have stud...

  1. Effect of substrate on the growth, nutritional and bioactive ...

    African Journals Online (AJOL)

    rosemary

    2016-07-06

    Jul 6, 2016 ... growth, determining nutritional and bioactive components of two oyster mushroom, Pleurotus ostreatus and. Pleurotus ... and the method of cultivation are of major importance ..... rendered alkaline with a few drops of ammonia solution. 5 ..... production and non-enzymatic antioxidant activity of Pleurotus.

  2. Bioactive Diterpenes and Sesquiterpenes from the Rhizomes of Wild ...

    African Journals Online (AJOL)

    Wild ginger (Siphonochilus aethiopicus (Schweinf) B.L Burtt) is used in traditional medicines in the West and South of Africa. In the present study, the crude hexane extract of wild ginger was evaluated for in vitro bioactivity. The components isolated from the plant for the first time are: epi-curzerenone, furanodienone ...

  3. Bioactive proanthocyanidins from the root bark of Cassia abbreviata ...

    African Journals Online (AJOL)

    Cassia abbreviata is an important medicinal plant used in the treatment of various infectious diseases. The ethnomedical efficacy of extracts of this plant species is attributed to its phytochemical constituents most of which are phenolics and anthraquinones. The aim of this study was to isolate and elucidate bioactive phenolic ...

  4. Application of magnetron sputtering for producing bioactive ceramic ...

    Indian Academy of Sciences (India)

    Wintec

    time is to coat the metal surface with a bioactive material that can promote rapid ... metal implant and the surrounding tissue because of their close similarity to the ... good control of coating composition, a good adhesion of the coating to the ...

  5. Excipient Nanoemulsions for Improving Oral Bioavailability of Bioactives

    Directory of Open Access Journals (Sweden)

    Laura Salvia-Trujillo

    2016-01-01

    Full Text Available The oral bioavailability of many hydrophobic bioactive compounds found in natural food products (such as vitamins and nutraceuticals in fruits and vegetables is relatively low due to their low bioaccessibility, chemical instability, or poor absorption. Most previous research has therefore focused on the design of delivery systems to incorporate isolated bioactive compounds into food products. However, a more sustainable and cost-effect approach to enhancing the functionality of bioactive compounds is to leave them within their natural environment, but specifically design excipient foods that enhance their bioavailability. Excipient foods typically do not have functionality themselves but they have the capacity to enhance the functionality of nutrients present in natural foods by altering their bioaccessibility, absorption, and/or chemical transformation. In this review article we present the use of excipient nanoemulsions for increasing the bioavailability of bioactive components from fruits and vegetables. Nanoemulsions present several advantages over other food systems for this application, such as the ability to incorporate hydrophilic, amphiphilic, and lipophilic excipient ingredients, high physical stability, and rapid gastrointestinal digestibility. The design, fabrication, and application of nanoemulsions as excipient foods will therefore be described in this article.

  6. BIOPEP database and other programs for processing bioactive peptide sequences.

    Science.gov (United States)

    Minkiewicz, Piotr; Dziuba, Jerzy; Iwaniak, Anna; Dziuba, Marta; Darewicz, Małgorzata

    2008-01-01

    This review presents the potential for application of computational tools in peptide science based on a sample BIOPEP database and program as well as other programs and databases available via the World Wide Web. The BIOPEP application contains a database of biologically active peptide sequences and a program enabling construction of profiles of the potential biological activity of protein fragments, calculation of quantitative descriptors as measures of the value of proteins as potential precursors of bioactive peptides, and prediction of bonds susceptible to hydrolysis by endopeptidases in a protein chain. Other bioactive and allergenic peptide sequence databases are also presented. Programs enabling the construction of binary and multiple alignments between peptide sequences, the construction of sequence motifs attributed to a given type of bioactivity, searching for potential precursors of bioactive peptides, and the prediction of sites susceptible to proteolytic cleavage in protein chains are available via the Internet as are other approaches concerning secondary structure prediction and calculation of physicochemical features based on amino acid sequence. Programs for prediction of allergenic and toxic properties have also been developed. This review explores the possibilities of cooperation between various programs.

  7. In vitro bioactivity and cytocompatibility of tricalcium silicate

    Indian Academy of Sciences (India)

    tricalcium silicate powder showed that it could induce bone- like apatite formation after ... ated by soaking them in SBF, cell adhesion and MTT assay, respectively. 2. .... tibility, which might be used as one of the bioactive coating materials and ...

  8. Therapeutic potential of dairy bioactive peptides: A contemporary perspective.

    Science.gov (United States)

    Sultan, Saira; Huma, Nuzhat; Butt, Masood Sadiq; Aleem, Muhammad; Abbas, Munawar

    2018-01-02

    Dairy products are associated with numerous health benefits. These are a good source of nutrients such as carbohydrates, protein (bioactive peptides), lipids, minerals, and vitamins, which are essential for growth, development, and maintenance of the human body. Accordingly, dairy bioactive peptides are one of the targeted compounds present in different dairy products. Dairy bioactive compounds can be classified as antihypertensive, anti-oxidative, immmunomodulant, anti-mutagenic, antimicrobial, opoid, anti-thrombotic, anti-obesity, and mineral-binding agents, depending upon biological functions. These bioactive peptides can easily be produced by enzymatic hydrolysis, and during fermentation and gastrointestinal digestion. For this reason, fermented dairy products, such as yogurt, cheese, and sour milk, are gaining popularity worldwide, and are considered excellent source of dairy peptides. Furthermore, fermented and non-fermented dairy products are associated with lower risks of hypertension, coagulopathy, stroke, and cancer insurgences. The current review article is an attempt to disseminate general information about dairy peptides and their health claims to scientists, allied stakeholders, and, certainly, readers.

  9. Bioactivity of mangrove humic materials on Rizophora mangle and ...

    African Journals Online (AJOL)

    Bioactivity of mangrove humic materials on Rizophora mangle and Laguncularia racemosa seedlings, Brazil. Leonardo Barros Dobbss, André Luiz Paier Barroso, Alessandro Coutinho Ramos, Karla Stéphanie Nunes Torrico, Fabíola Schunk de Souza Arçari, Daniel Basílio Zandonadi ...

  10. Ethnobotany, phytochemistry, and bioactivity of the genus Turnera (Passifloraceae) with a focus on damiana--Turnera diffusa.

    Science.gov (United States)

    Szewczyk, Katarzyna; Zidorn, Christian

    2014-03-28

    Turnera, and experimentally documented bioactivities from Turnera extracts and pure compounds derived from Turnera extracts are compiled. Moreover, some of the most interesting avenues for future research projects are being discussed briefly. These include in particular the aphrodisiac activity of Turnera diffusa and the antibiotic activity potentiating effect of Turnera ulmifolia L. against aminoglycoside resistant bacteria. Copyright © 2014 Elsevier Ireland Ltd. All rights reserved.

  11. The Influence of Different Air-Drying Conditions on Bioactive Compounds and Antioxidant Activity of Berries.

    Science.gov (United States)

    Bustos, Mariela C; Rocha-Parra, Diego; Sampedro, Ines; de Pascual-Teresa, Sonia; León, Alberto E

    2018-03-21

    The aim of the present research was to study the effect of convective drying on color, bioactive compounds, and antioxidant activity of berry fruits and to chemically characterize the polyphenolic composition of raspberry, boysenberry, redcurrants, and blackcurrants fruit. Drying berries at 65 °C provoked the best conservations of color, particularly for boysenberry and blackcurrant. Drying at 65 °C was also the condition that showed higher level of polyphenols, while drying at 50 or 130 °C showed above % degradation of them due to the long time or high temperature drying. Radical scavenging activity was the predominant antioxidant mechanism in all samples, with 65 °C dried berries being the most active ones possibly because of polyphenol depolymerization. The anthocyanin profile showed that delphinidin and cyanidin derivatives were the most abundant anthocyanidins with different predominance between berry genera. Degradation of anthocyanins was increased with drying temperature been Cy 3-glucoside and Cy 3-rutinoside the most abundant.

  12. Metabolic profile of the bioactive compounds of burdock (Arctium lappa) seeds, roots and leaves.

    Science.gov (United States)

    Ferracane, Rosalia; Graziani, Giulia; Gallo, Monica; Fogliano, Vincenzo; Ritieni, Alberto

    2010-01-20

    In this work the bioactive metabolic profile, the antioxidant activity and total phenolic content of burdock (Arctium lappa) seeds, leaves and roots were obtained. TEAC values and total phenolic content for hydro-alcoholic extracts of burdock ranged from 67.39 to 1.63 micromol Trolox equivalent/100g dry weight (DW), and from 2.87 to 45 g of gallic acid equivalent/100g DW, respectively. Phytochemical compounds were analyzed by liquid chromatography coupled to electrospray tandem mass spectrometry (LC/MS/MS) in negative mode. The main compounds of burdock extracts were caffeoylquinic acid derivatives, lignans (mainly arctiin) and various flavonoids. The occurrence of some phenolic acids (caffeic acid, chlorogenic acid and cynarin) in burdock seeds; arctiin, luteolin and quercetin rhamnoside in burdock roots; phenolic acids, quercetin, quercitrin and luteolin in burdock leaves was reported for the first time.

  13. Red Maple (Acer rubrum) Aerial Parts as a Source of Bioactive Phenolics.

    Science.gov (United States)

    Zhang, Yan; Ma, Hang; Yuan, Tao; Seeram, Navindra P

    2015-08-01

    The bark and stems of red maple (Acer rubrum) are reported to contain bioactive phenolics but its aerial parts, namely, flowers and leaves, remain largely unexplored. This is unfortunate considering that various parts of the red maple were used for traditional medicinal purposes by the indigenous peoples of eastern North America, where this species is found. Herein, we report the identification of twenty-five (1-25) phenolics, including two new galloyl derivatives (1 and 2), from red maple flowers and leaves. Of these, ten compounds (1-10), including the new compounds, were isolated and identified by NMR and HRESIMS data while the remaining fifteen compounds (11-25) were identified by HPLC-DAD analyses (by comparison with chemical standards). The isolates (1-10), along with the clinical drug, acarbose, were evaluated for their alpha-glucosidase enzyme inhibitory activities.

  14. Molecular characteristics of humic acids isolated from vermicomposts and their relationship to bioactivity.

    Science.gov (United States)

    Martinez-Balmori, Dariellys; Spaccini, Riccardo; Aguiar, Natália Oliveira; Novotny, Etelvino Henrique; Olivares, Fábio Lopes; Canellas, Luciano Pasqualoto

    2014-11-26

    Vermitechnology is an effective composting method, which transforms biomass into nutrient-rich organic fertilizer. Mature vermicompost is a renewable organic product containing humic substances with high biological activity. The aim of this study was to assess the chemical characteristics and the bioactivity of humic acids isolated from different vermicomposts produced with either cattle manure, sugar cane bagasse, sunflower cake from seed oil extraction, or filter cake from a sugar cane factory. More than 200 different molecules were found, and it was possible to identify chemical markers on humic acids according to the nature of the organic source. The large hydrophobic character of humic extracts and the preservation of altered lignin derivatives confer to humic acids the ability to induce lateral root emergence in maize seedlings. Humic acid-like substances extracted from plant biomass residues represent an additional valuable product of vermicomposting that can be used as a plant growth promoter.

  15. Marine Polysaccharides: A Source of Bioactive Molecules for Cell Therapy and Tissue Engineering

    Directory of Open Access Journals (Sweden)

    Anne-Marie Fischer

    2011-09-01

    Full Text Available The therapeutic potential of natural bioactive compounds such as polysaccharides, especially glycosaminoglycans, is now well documented, and this activity combined with natural biodiversity will allow the development of a new generation of therapeutics. Advances in our understanding of the biosynthesis, structure and function of complex glycans from mammalian origin have shown the crucial role of this class of molecules to modulate disease processes and the importance of a deeper knowledge of structure-activity relationships. Marine environment offers a tremendous biodiversity and original polysaccharides have been discovered presenting a great chemical diversity that is largely species specific. The study of the biological properties of the polysaccharides from marine eukaryotes and marine prokaryotes revealed that the polysaccharides from the marine environment could provide a valid alternative to traditional polysaccharides such as glycosaminoglycans. Marine polysaccharides present a real potential for natural product drug discovery and for the delivery of new marine derived products for therapeutic applications.

  16. Exopolysaccharide from Ganoderma applanatum as a Promising Bioactive Compound with Cytostatic and Antibacterial Properties

    Science.gov (United States)

    Osińska-Jaroszuk, Monika; Błachowicz, Adriana; Wydrych, Jerzy; Polak, Jolanta; Jarosz-Wilkołazka, Anna; Kandefer-Szerszeń, Martyna

    2014-01-01

    A new exopolysaccharide preparation isolated from stationary cultures of the white rot fungus Ganoderma applanatum (GpEPS) was tested in terms of its bioactive properties including its cytotoxic and immunostimulatory effect. The results indicate that the tested GpEPS (at concentrations above 22.85 µg/mL and 228.5 µg/mL) may exhibit selective activity against tumor cells (cell lines SiHa) and stimulate production of TNF-α THP-1-derived macrophages at the level of 752.17 pg/mL. The GpEPS showed antibacterial properties against Staphyloccoccus aureus and a toxic effect against Vibrio fischeri cells (82.8% cell damage). High cholesterol-binding capacity and triglycerides-binding capacity (57.9% and 41.6% after 24 h of incubation with the tested substances, resp.) were also detected for the investigated samples of GpEPS. PMID:25114920

  17. BIOACTIVE PEPTIDES OF THE COW MILK WHEY PROTEINS (Bos taurus

    Directory of Open Access Journals (Sweden)

    A. V. Iukalo

    2013-10-01

    Full Text Available Data on the biological functions of milk whey proteins, which are implemented at the level of their proteolytic degradation products — bioactive peptides have been reviewed. The main functions of these proteins is to provide the amino acid nutrition of mammals in the early stages of development, as well as the transport of fatty acids, retinol, involved in the synthesis of lactose, ions of calcium and iron, immune protection, antimicrobial action, etc. However, in recent years, it has been found that milk proteins like casein are precursors of biologically active peptides. Аngiotensin — converting enzyme, opioid peptides which are opiate receptor agonists, anti–microbial peptides, peptides with immunomodulatory and hypocholesterolemic action, and peptides affecting motility have been found among the products of proteolytic degradation of ?-lactoglobulin, ?-laktoalbumin, lactoferrin and milk whey albumin. Also data on the possible participation of peptides from milk whey proteins in the implementation of the biological functions of both the assimilation of calcium, antioxidant effect, the regulation of appetite, anticarcinogenic are provided. The authors assume that the phenomenon of bioactive peptides formation could be considered as an additional function of natural food proteins, which gives advantages to the mammals and has a positive effect on their development in the postnatal period. Ways of bioactive peptides formation, their resistance to action of proteolytic enzymes, the ability to cross into the bloodstream and have biological effects have been also discussed. Up to date, only a few products with bioactive peptides from milk whey proteins are obtained. Further studies of their structure, mechanism of action, ways of formation and methods of isolation are required for their wider use. Formation of functional products based on bioactive peptides from milk whey proteins will allow efficient use of milk whey, which is often a

  18. Derivative chameleons

    International Nuclear Information System (INIS)

    Noller, Johannes

    2012-01-01

    We consider generalized chameleon models where the conformal coupling between matter and gravitational geometries is not only a function of the chameleon field φ, but also of its derivatives via higher order co-ordinate invariants (such as ∂ μ φ∂ μ φ,□φ,...). Specifically we consider the first such non-trivial conformal factor A(φ,∂ μ φ∂ μ φ). The associated phenomenology is investigated and we show that such theories have a new generic mass-altering mechanism, potentially assisting the generation of a sufficiently large chameleon mass in dense environments. The most general effective potential is derived for such derivative chameleon setups and explicit examples are given. Interestingly this points us to the existence of a purely derivative chameleon protected by a shift symmetry for φ → φ+c. We also discuss potential ghost-like instabilities associated with mass-lifting mechanisms and find another, mass-lowering and instability-free, branch of solutions. This suggests that, barring fine-tuning, stable derivative models are in fact typically anti-chameleons that suppress the field's mass in dense environments. Furthermore we investigate modifications to the thin-shell regime and prove a no-go theorem for chameleon effects in non-conformal geometries of the disformal type

  19. Derivative chameleons

    Energy Technology Data Exchange (ETDEWEB)

    Noller, Johannes, E-mail: johannes.noller08@imperial.ac.uk [Theoretical Physics, Blackett Laboratory, Imperial College London, Prince Consort Road, London, SW7 2BZ (United Kingdom)

    2012-07-01

    We consider generalized chameleon models where the conformal coupling between matter and gravitational geometries is not only a function of the chameleon field φ, but also of its derivatives via higher order co-ordinate invariants (such as ∂{sub μ}φ∂{sup μ}φ,□φ,...). Specifically we consider the first such non-trivial conformal factor A(φ,∂{sub μ}φ∂{sup μ}φ). The associated phenomenology is investigated and we show that such theories have a new generic mass-altering mechanism, potentially assisting the generation of a sufficiently large chameleon mass in dense environments. The most general effective potential is derived for such derivative chameleon setups and explicit examples are given. Interestingly this points us to the existence of a purely derivative chameleon protected by a shift symmetry for φ → φ+c. We also discuss potential ghost-like instabilities associated with mass-lifting mechanisms and find another, mass-lowering and instability-free, branch of solutions. This suggests that, barring fine-tuning, stable derivative models are in fact typically anti-chameleons that suppress the field's mass in dense environments. Furthermore we investigate modifications to the thin-shell regime and prove a no-go theorem for chameleon effects in non-conformal geometries of the disformal type.

  20. Electricity derivatives

    CERN Document Server

    Aïd, René

    2015-01-01

    Offering a concise but complete survey of the common features of the microstructure of electricity markets, this book describes the state of the art in the different proposed electricity price models for pricing derivatives and in the numerical methods used to price and hedge the most prominent derivatives in electricity markets, namely power plants and swings. The mathematical content of the book has intentionally been made light in order to concentrate on the main subject matter, avoiding fastidious computations. Wherever possible, the models are illustrated by diagrams. The book should allow prospective researchers in the field of electricity derivatives to focus on the actual difficulties associated with the subject. It should also offer a brief but exhaustive overview of the latest techniques used by financial engineers in energy utilities and energy trading desks.

  1. In vitro study of polycaprolactone/bioactive glass composite coatings on corrosion and bioactivity of pure Mg

    Energy Technology Data Exchange (ETDEWEB)

    Yang, Yuyun; Michalczyk, Carolin [Institute of Biomaterials, University of Erlangen-Nuremberg, 91058 Erlangen (Germany); Singer, Ferdinand [Institute of Surface Science and Corrosion, University of Erlangen-Nuremberg, 91058 Erlangen (Germany); Virtanen, Sannakaisa, E-mail: virtanen@ww.uni-erlangen.de [Institute of Surface Science and Corrosion, University of Erlangen-Nuremberg, 91058 Erlangen (Germany); Boccaccini, Aldo R., E-mail: aldo.boccaccini@ww.uni-erlangen.de [Institute of Biomaterials, University of Erlangen-Nuremberg, 91058 Erlangen (Germany)

    2015-11-15

    Highlights: • Bioactive glass nanoparticles (nBG) enhance bioactivity of PCL coatings on Mg. • Barrier properties of PCL can be altered by nBG addition. • Degradation of PCL increased by addition of nBG. - Abstract: The influence of the addition of nano-scaled bioactive glass (nBG) powder into polycaprolactone (PCL) coatings on the biodegradation and bioactivity of pure Mg was investigated in the present work. Scanning electron microscopy (SEM), energy-dispersive X-ray spectrometry (EDS), Fourier transform infrared spectroscopy (FTIR) and electrochemical methods were employed to characterize the morphology, chemical composition and anticorrosion properties of the coatings. The results indicate that nBG addition in PCL increases the degradation of PCL in physiological solution; depending on the amount of nBG in the composite coating, the barrier properties of PCL therefore can be modified. At the same time, the addition of nBG facilitates the formation of hydroxyapatite during 7 days immersion in simulated body fluid (SBF).

  2. Controlled release of bioactive PDGF-AA from a hydrogel/nanoparticle composite.

    Science.gov (United States)

    Elliott Donaghue, Irja; Shoichet, Molly S

    2015-10-01

    Polymer excipients, such as low molar mass poly(ethylene glycol) (PEG), have shown contradictory effects on protein stability when co-encapsulated in polymeric nanoparticles. To gain further insight into these effects, platelet-derived growth factor (PDGF-AA) was encapsulated in polymeric nanoparticles with vs. without PEG. PDGF-AA is a particularly compelling protein, as it has been demonstrated to promote cell survival and induce the oligodendrocyte differentiation of neural stem/progenitor cells (NSPCs) both in vitro and in vivo. Here we show, for the first time, the controlled release of bioactive PDGF-AA from an injectable nanoparticle/hydrogel drug delivery system (DDS). PDGF-AA was encapsulated, with high efficiency, in poly(lactide-co-glycolide) nanoparticles, and its release from the drug delivery system was followed over 21 d. Interestingly, the co-encapsulation of low molecular weight poly(ethylene glycol) increased the PDGF-AA loading but, unexpectedly, accelerated the aggregation of PDGF-AA, resulting in reduced activity and detection by enzyme-linked immunosorbent assay (ELISA). In the absence of PEG, released PDGF-AA remained bioactive as demonstrated with NSPC oligodendrocyte differentiation, similar to positive controls, and significantly different from untreated controls. This work presents a novel delivery method for differentiation factors, such as PDGF-AA, and provides insights into the contradictory effects reported in the literature of excipients, such as PEG, on the loading and release of proteins from polymeric nanoparticles. Previously, the polymer poly(ethylene glycol) (PEG) has been used in many biomaterials applications, from surface coatings to the encapsulation of proteins. In this work, we demonstrate that, unexpectedly, low molecular weight PEG has a deleterious effect on the release of the encapsulated protein platelet-derived growth factor AA (PDGF-AA). We also demonstrate release of bioactive PDGF-AA (in the absence of PEG

  3. Identification, Bioactivity, and Productivity of Actinomycins from the Marine-Derived Streptomyces heliomycini

    Directory of Open Access Journals (Sweden)

    Dongyang Wang

    2017-06-01

    Full Text Available In the process of profiling the secondary metabolites of actinobacteria isolated from the Saudi coastal habitats for production of antibiotics and anti-cancer drugs, the cultures of strain WH1 that was identified as Streptomyces heliomycini exhibited strong antibacterial activity against Staphylococcus aureus. By means of MS and NMR techniques, the active compounds were characterized as actinomycins X0β, X2, and D, respectively. The research on the productivity of this strain for actinomycins revealed that the highest production of actinomycins X0β, X2, and D was reached in the medium MII within 5% salinity and pH 8.5. In this optimized condition, the fermentation titers of actinomycins X0β, X2, and D were 107.6 ± 4.2, 283.4 ± 75.3, and 458.0 ± 76.3 mg/L, respectively. All the three actinomycins X0β, X2, and D showed potent cytotoxicities against the MCF-7, K562, and A549 tumor cell lines, in which actinomycin X2 was the most active against the three tumor cell lines with the IC50 values of 0.8–1.8 nM. Both actinomycins X2 and D showed potent antibacterial activities against S. aureus and the methicillin-resistant S. aureus, Bacillus subtilis, and B. cereus and the actinomycin X2 was more potent.

  4. New bioactive hydrogenated linderazulene-derivatives from the gorgonian Echinogorgia complexa

    Digital Repository Service at National Institute of Oceanography (India)

    Manzo, E.; Ciavatta, M.L.; Gresa, M.P.L.; Gavagnin, M.; Villani, G.; Naik, C; Cimino, G.

    Chemical analysis of the secondary metabolite pattern of the gorgonian Echinogorgia complexa, collected along South Indian coasts, showed the presence of two new tricyclic guaiane furanosesquiterpenes, iso-echinofuran (3) and 8,9-dihydro...

  5. Production of monosaccharides and bio-active compounds derived from marine polysaccharides using subcritical water hydrolysis.

    Science.gov (United States)

    Meillisa, Aviannie; Woo, Hee-Chul; Chun, Byung-Soo

    2015-03-15

    Polysaccharides are the major components of brown seaweed, accounting for approximately 40-65% of the total mass. The majority of the brown seaweed polysaccharides consists of alginate (40% of dry matter), a linear hetero-polysaccharides commonly developed in fields. However, depolymerisation of alginate is required to recover high-value compounds. In this report, depolymerisation was performed using subcritical water hydrolysis (SWH) at 180-260°C, with a ratio of material to water of 1:25 (w/v) and 1% formic acid as a catalyst. Sugar recovery was higher at low temperatures in the presence of catalyst. The antioxidant properties of Saccharina japonica showed the best activity at 180°C in the presence of a catalyst. The mass spectra produced using MALDI-TOF showed that polysaccharides and oligosaccharides were produced during hydrothermal treatment. Hydrolysis treatment at 180°C in the presence of a catalyst may be useful for modifying the structure of S. japonica and purified alginate. Copyright © 2014 Elsevier Ltd. All rights reserved.

  6. Triazole-curcuminoids: A new class of derivatives for 'tuning' curcumin bioactivities?

    Science.gov (United States)

    Caprioglio, Diego; Torretta, Simone; Ferrari, Maila; Travelli, Cristina; Grolla, Ambra A; Condorelli, Fabrizio; Genazzani, Armando A; Minassi, Alberto

    2016-01-15

    Curcumin is a unique blend of pharmacophores responsible for the pleiotropy of this natural pigment. In the present study we have replaced the 1,3-dicarbonyl moiety with a 1,2,3-triazole ring to furnish a new class of triazole-curcuminoids as a possible strategy to generate new compounds with different potency and selectivity compared to curcumin. We obtained a proof-of-principle library of 28 compounds tested for their cytotoxicity (SY-SY5Y and HeLa cells) and for their ability to inhibit NF-κB. Furthermore, we also generated 1,3-dicarbonyl curcuminoids of selected click compounds. Triazole-curcuminoids lost their ability to be Michael's acceptors, yet maintained some of the features of the parent compounds and disclosed new ones. In particular, we found that some compounds were able to inhibit NF-κB without showing cytotoxicity, while others, unlike curcumin, activated NF-κB signalling. This validates the hypothesis that click libraries can be used to investigate the biological activities of curcumin as well as generate analogs with selected features. Copyright © 2015 Elsevier Ltd. All rights reserved.

  7. Screening concepts, characterization and structural analysis of microbial-derived bioactive lipopeptides: a review.

    Science.gov (United States)

    Biniarz, Piotr; Łukaszewicz, Marcin; Janek, Tomasz

    2017-05-01

    Lipopeptide biosurfactants are surface active biomolecules that are produced by a variety of microorganisms. Microbial lipopeptides have gained the interest of microbiologists, chemists and biochemists for their high biodiversity as well as efficient action, low toxicity and good biodegradability in comparison to synthetic counterparts. In this report, we review methods for the production, isolation and screening, purification and structural characterization of microbial lipopeptides. Several techniques are currently available for each step, and we describe the most commonly utilized and recently developed techniques in this review. Investigations on lipopeptide biosurfactants in natural products require efficient isolation techniques for the characterization and evaluation of chemical and biological properties. A combination of chromatographic and spectroscopic techniques offer opportunities for a better characterization of lipopeptide structures, which in turn can lead to the application of lipopeptides in food, pharmaceutical, cosmetics, agricultural and bioremediation industries.

  8. Anaerobes as Sources of Bioactive Compounds and Health Promoting Tools.

    Science.gov (United States)

    Mamo, Gashaw

    Aerobic microorganisms have been sources of medicinal agents for several decades and an impressive variety of drugs have been isolated from their cultures, studied and formulated to treat or prevent diseases. On the other hand, anaerobes, which are believed to be the oldest life forms on earth and evolved remarkably diverse physiological functions, have largely been neglected as sources of bioactive compounds. However, results obtained from the limited research done so far show that anaerobes are capable of producing a range of interesting bioactive compounds that can promote human health. In fact, some of these bioactive compounds are found to be novel in their structure and/or mode of action.Anaerobes play health-promoting roles through their bioactive products as well as application of whole cells. The bioactive compounds produced by these microorganisms include antimicrobial agents and substances such as immunomodulators and vitamins. Bacteriocins produced by anaerobes have been in use as preservatives for about 40 years. Because these substances are effective at low concentrations, encounter relatively less resistance from bacteria and are safe to use, there is a growing interest in these antimicrobial agents. Moreover, several antibiotics have been reported from the cultures of anaerobes. Closthioamide and andrimid produced by Clostridium cellulolyticum and Pantoea agglomerans, respectively, are examples of novel antibiotics of anaerobe origin. The discovery of such novel bioactive compounds is expected to encourage further studies which can potentially lead to tapping of the antibiotic production potential of this fascinating group of microorganisms.Anaerobes are widely used in preparation of fermented foods and beverages. During the fermentation processes, these organisms produce a number of bioactive compounds including anticancer, antihypertensive and antioxidant substances. The well-known health promoting effect of fermented food is mostly due to these

  9. Functionally graded bioactive coatings: From fabrication to testing

    Science.gov (United States)

    Foppiano, Silvia

    Every year about half a million Americans undergo total joint replacement surgery of some kind. This number is expected to steadily increase in the future. About 20% of these patients will need a revision surgery because of implant failure, with a significant increase in health care cost. Current implant materials for load bearing applications must be strong enough to support the loads involved in daily activities, and bioinert, to limit reactivity in the body that may cause inflammatory and other adverse reactions. Metal alloys are typically used as materials for load bearing implants and rely on mechanical interlocking to achieve fixation which can be improved by using bone cements. To improve implant osteointegration, metal implants have been coated with a bone-like mineral: hydroxyapatite (HA). The plasma spray technique is commonly used to apply the HA coating. Such implants do not require the use of bone cement. Plasma sprayed HA coated implants are FDA approved and currently on the market, but their properties are not reproducible or reliable. Thus, coating delamination can occur. Our research group developed a novel family of bioactive glasses which were enameled onto titanium alloy using a functionally graded approach. We stratified the coating with different glass compositions to fulfill different functions. We coupled a first glass layer, with a good CTE match to the alloy, with a second layer of bioactive glass obtaining a functionally graded bioactive coating (FGC). In this thesis for the first time the cytocompatibility of novel bioactive glasses, and their functionally graded coatings on Ti6Al4V, was studied with an in vitro bone model (MC3T3-E1.4 mouse preosteblast cells). The novel bioactive glasses are cytocompatible and no compositional change is required. The fabrication process is reproducible, introduces a small (average 6 vol%) amount of crystallization, which does not significantly affect bioactivity in SBF as tested. The coatings are

  10. Alkali-free bioactive glasses for bone regeneration =

    Science.gov (United States)

    Kapoor, Saurabh

    Bioactive glasses and glass-ceramics are a class of third generation biomaterials which elicit a special response on their surface when in contact with biological fluids, leading to strong bonding to living tissues. The purpose of the present study was to develop diopside based alkali-free bioactive glasses in order to achieve good sintering behaviour, high bioactivity, and a dissolution/ degradation rates compatible with the target applications in bone regeneration and tissue engineering. Another aim was to understand the structure-property relationships in the investigated bioactive glasses. In this quest, various glass compositions within the Diopside (CaMgSi2O6) - Fluorapatite (Ca5(PO4)3F) - Tricalcium phosphate (3CaO•P2O5) system have been investigated. All the glasses were prepared by melt-quenching technique and characterized by a wide array of complementary characterization techniques. The glass-ceramics were produced by sintering of glass powders compacts followed by a suitable heat treatment to promote the nucleation and crystallization phenomena. Furthermore, selected parent glass compositions were doped with several functional ions and an attempt to understand their effects on the glass structure, sintering ability and on the in vitro bio-degradation and biomineralization behaviours of the glasses was made. The effects of the same variables on the devitrification (nucleation and crystallization) behaviour of glasses to form bioactive glass-ceramics were also investigated. Some of the glasses exhibited high bio-mineralization rates, expressed by the formation of a surface hydroxyapatite layer within 1-12 h of immersion in a simulated body fluid (SBF) solution. All the glasses showed relatively lower degradation rates in comparison to that of 45S5 Bioglass. Some of the glasses showed very good in vitro behaviour and the glasses co-doped with zinc and strontium showed an in vitro dose dependent behaviour. The as-designed bioactive glasses and glass

  11. The Stability of Bioactive Compounds in Spaceflight Foods

    Science.gov (United States)

    Cooper, M. R.; Douglas, G. L.

    2017-01-01

    The status and stability of bioactive compounds in the processed and shelf-stable spaceflight food system have not previously been investigated though the presence of such compounds in aged space foods could have health significance for crews on long duration exploration missions. Over forty foods - either existing International Space Station (ISS) food provisioning items, newly developed foods for spaceflight, or commercially-available ready-to-eat foods - that were predicted to have a relatively high concentrations of one or more bioactive compounds (lycopene, lutein, omega-3 fatty acids, phenolics, sterols, and/or flavonoids) were selected for the study. Food samples were sent overnight to the Food Composition Laboratory of the Linus Pauling Institute at Oregon State University (Corvallis, OR) for bioactive compound analysis. Three packages of each product were blended together for the analysis to reduce package-to-package variability. All ISS food items and commercial foods were analyzed initially and after 12 and 24 months of 21degC storage. Food development occurred in a staggered fashion, so data collection for the newly developed foods continues. Lastly, sensory evaluation and additional temperature storage data (4degC, 35degC) for select foods were collected to establish additional stability parameters. Efficacious concentrations of lycopene, lutein, and omega-3 fatty acids were measured in limited spaceflight foods; two grams of sterols a day may be difficult to achieve with the current space diet. Total polyphenol delivery appears stable and adequate, but individual phenolic compounds vary in stability and were not specifically evaluated in this study. The data suggests that some bioactive compounds, like lycopene and lutein, degrade and then plateau at some equilibrium concentration. The anthocyanin stability appears to be related to storage temperature and food matrix, and lutein stability in leafy vegetables may be impacted by storage temperature

  12. Peptide Fractions Obtained from Rice By-Products by Means of an Environment-Friendly Process Show In Vitro Health-Related Bioactivities.

    Science.gov (United States)

    Ferri, Maura; Graen-Heedfeld, Jürgen; Bretz, Karlheinz; Guillon, Fabien; Michelini, Elisa; Calabretta, Maria Maddalena; Lamborghini, Matteo; Gruarin, Nicolò; Roda, Aldo; Kraft, Axel; Tassoni, Annalisa

    2017-01-01

    Recently, the isolation of new health-related bioactive molecules derived from agro-food industrial by-products by means of environment-friendly extraction processes has become of particular interest. In the present study, a protein by-product from the rice starch industry was hydrolysed with five commercial proteolytic enzymes, avoiding the use of solvents or chemicals. The digestion processes were optimised, and the digestates were separated in fractions with four different molecular weight ranges by using a cross-flow membrane filtration technique. Total hydrolysates and fractions were tested in vitro for a wide range of biological activities. For the first time rice-derived peptides were assayed for anti-tyrosinase, anti-inflammatory, cytotoxicity and irritation capacities. Antioxidant and anti-hypertensive activities were also evaluated. Protamex, Alcalase and Neutrase treatments produced peptide fractions with valuable bioactivities without resulting cytotoxic or irritant. Highest levels of bioactivity were detected in Protamex-derived samples, followed by samples treated with Alcalase. Based on the present results, a future direct exploitation of isolated peptide fractions in the nutraceutical, functional food and cosmetic industrial fields may be foreseen.

  13. Peptide Fractions Obtained from Rice By-Products by Means of an Environment-Friendly Process Show In Vitro Health-Related Bioactivities.

    Directory of Open Access Journals (Sweden)

    Maura Ferri

    Full Text Available Recently, the isolation of new health-related bioactive molecules derived from agro-food industrial by-products by means of environment-friendly extraction processes has become of particular interest. In the present study, a protein by-product from the rice starch industry was hydrolysed with five commercial proteolytic enzymes, avoiding the use of solvents or chemicals. The digestion processes were optimised, and the digestates were separated in fractions with four different molecular weight ranges by using a cross-flow membrane filtration technique. Total hydrolysates and fractions were tested in vitro for a wide range of biological activities. For the first time rice-derived peptides were assayed for anti-tyrosinase, anti-inflammatory, cytotoxicity and irritation capacities. Antioxidant and anti-hypertensive activities were also evaluated. Protamex, Alcalase and Neutrase treatments produced peptide fractions with valuable bioactivities without resulting cytotoxic or irritant. Highest levels of bioactivity were detected in Protamex-derived samples, followed by samples treated with Alcalase. Based on the present results, a future direct exploitation of isolated peptide fractions in the nutraceutical, functional food and cosmetic industrial fields may be foreseen.

  14. Anti-cancer activities of diospyrin, its derivatives and analogues

    KAUST Repository

    Sagar, Sunil

    2010-09-01

    Natural products have played a vital role in drug discovery and development process for cancer. Diospyrin, a plant based bisnaphthoquinonoid, has been used as a lead molecule in an effort to develop anti-cancer drugs. Several derivatives/analogues have been synthesized and screened for their pro-apoptotic/anti-cancer activities so far. Our review is focused on the pro-apoptotic/anti-cancer activities of diospyrin, its derivatives/analogues and the different mechanisms potentially involved in the bioactivity of these compounds. Particular focus has been placed on the different mechanisms (both chemical and molecular) thought to underlie the bioactivity of these compounds. A brief bioinformatics analysis at the end of the article provides novel insights into the new potential mechanisms and pathways by which these compounds might exert their effects and lead to a better realization of the full therapeutic potential of these compounds as anti-cancer drugs. © 2010 Elsevier Masson SAS. All rights reserved.

  15. Anti-cancer activities of diospyrin, its derivatives and analogues

    KAUST Repository

    Sagar, Sunil; Kaur, Mandeep; Minneman, Kenneth P.; Bajic, Vladimir B.

    2010-01-01

    Natural products have played a vital role in drug discovery and development process for cancer. Diospyrin, a plant based bisnaphthoquinonoid, has been used as a lead molecule in an effort to develop anti-cancer drugs. Several derivatives/analogues have been synthesized and screened for their pro-apoptotic/anti-cancer activities so far. Our review is focused on the pro-apoptotic/anti-cancer activities of diospyrin, its derivatives/analogues and the different mechanisms potentially involved in the bioactivity of these compounds. Particular focus has been placed on the different mechanisms (both chemical and molecular) thought to underlie the bioactivity of these compounds. A brief bioinformatics analysis at the end of the article provides novel insights into the new potential mechanisms and pathways by which these compounds might exert their effects and lead to a better realization of the full therapeutic potential of these compounds as anti-cancer drugs. © 2010 Elsevier Masson SAS. All rights reserved.

  16. Preparation of bioactive porous HA/PCL composite scaffolds

    Energy Technology Data Exchange (ETDEWEB)

    Zhao, J.; Guo, L.Y.; Yang, X.B. [Key Laboratory of Advanced Technologies of Materials (Ministry of Education), School of Materials Science and Engineering, Southwest Jiaotong University, Chengdu 610031 (China); Weng, J. [Key Laboratory of Advanced Technologies of Materials (Ministry of Education), School of Materials Science and Engineering, Southwest Jiaotong University, Chengdu 610031 (China)], E-mail: jweng@swjtu.cn

    2008-12-30

    Porous hydroxyapatite (HA) bioceramic scaffold has been widely attracted the attention to act as a three-dimensional (3D) template for cell adhesion, proliferation, differentiation and thus promoting bone and cartilage regeneration because of its osteoinduction. However, the porous bioceramic scaffold is fragile so that it is not suitable to be applied in clinic for bone repair or replacement. Therefore, it is significant to improve the mechanical property of porous HA bioceramics while the interconnected structure is maintained for tissue ingrowth in vivo. In the present research, a porous composite scaffold composed of HA scaffold and polycaprolactone (PCL) lining was fabricated by the method of polymer impregnating to produce HA scaffold coated with PCL lining. Subsequently, the composite scaffolds were deposited with biomimetic coating for improving the bioactivity. The HA/PCL composite scaffolds with improved mechanical property and bioactivity is expected to be a promising bone substitute in tissue engineering applications.

  17. Essential oils: extraction, bioactivities, and their uses for food preservation.

    Science.gov (United States)

    Tongnuanchan, Phakawat; Benjakul, Soottawat

    2014-07-01

    Essential oils are concentrated liquids of complex mixtures of volatile compounds and can be extracted from several plant organs. Essential oils are a good source of several bioactive compounds, which possess antioxidative and antimicrobial properties. In addition, some essential oils have been used as medicine. Furthermore, the uses of essential oils have received increasing attention as the natural additives for the shelf-life extension of food products, due to the risk in using synthetic preservatives. Essential oils can be incorporated into packaging, in which they can provide multifunctions termed "active or smart packaging." Those essential oils are able to modify the matrix of packaging materials, thereby rendering the improved properties. This review covers up-to-date literatures on essential oils including sources, chemical composition, extraction methods, bioactivities, and their applications, particularly with the emphasis on preservation and the shelf-life extension of food products. © 2014 Institute of Food Technologists®

  18. Chemistry and Functionality of Bioactive Compounds Present in Persimmon

    Directory of Open Access Journals (Sweden)

    Shazia Yaqub

    2016-01-01

    Full Text Available Extensive research has related the consumption of persimmon with the reduced risk of various diseases and particularly highlighted the presence of bioactive phenolic compounds for their therapeutic properties. Major phenolic compounds present in persimmon are ferulic acid, p-coumaric acid, and gallic acid. β-Cryptoxanthin, lycopene, β-carotene, zeaxanthin, and lutein are important carotenoids having antioxidant potential. They are important to prevent oxidation of low-density lipoproteins, safeguard beta cells of the pancreas, and reduce cardiovascular diseases, cancer, diabetes mellitus, and damage caused by chronic alcohol consumption. In this paper, the chemistry and health benefits of bioactive compounds present in persimmon are reviewed to encourage impending applications and to facilitate further research activities.

  19. Interstitial fluid contains higher in vitro IGF bioactivity than serum

    DEFF Research Database (Denmark)

    Espelund, Ulrick; Søndergaard, Klaus; Bjerring, Peter

    2012-01-01

    MEASURE: Serum and SBF concentrations of bioactive IGF (determined in vitro by specific IGF-I receptor (IGF-IR) phosphorylation assay), immunoreactive IGF and IGF binding protein (IGFBP) levels, Western ligand blotting (WLB) of IGFBPs and IGFBP-3 Western immunoblotting (WiB). RESULTS: The ability of SBF...... to phosphorylate the IGF-IR in vitro was 41±27% higher than that of serum (P=0.007 by repeated measures ANOVA). By contrast, immunoreactive IGF and IGFBP-concentrations were approximately 50% lower in SBF than in serum (all P≤0.002). A marked difference in the composition of IGFBPs between serum and SBF...... was observed, including 3-fold elevated amounts of IGFBP-3 fragments in SBF (Pvitro IGF bioactivity was higher in SBF than in serum. This may...

  20. Bioactive compounds of sea cucumbers and their therapeutic effects

    Science.gov (United States)

    Shi, Shujuan; Feng, Wenjing; Hu, Song; Liang, Shixiu; An, Nina; Mao, Yongjun

    2016-05-01

    Sea cucumbers belong to the Class Holothuroidea of marine invertebrates. They are commercially valuable and prized as a food and folk medicine in Asia. Nutritionally, sea cucumbers have an impressive profile of valuable nutrients such as vitamins, minerals and amino acids. A number of unique biological and pharmacological activities/properties, including anticancer, anticoagulant/antithrombotic, antimicrobial, antioxidant, antihyperlipidemic, antihyperglycemic, anti-inflammatory, antihypertension and radioprotective, have been ascribed to various compounds isolated from sea cucumbers. The therapeutic properties and medicinal benefits of sea cucumbers can be linked to the presence of a wide array of bioactives, especially triterpene glycosides, acid mucopolysaccharide, sphingoid bases, glycolipids, fucosylated chondroitin sulfate, polysaccharides, phospholipids, cerebrosides, phosphatidylcholines, and other extracts and hydrolysates. This review highlights the valuable bioactive components as well as the multiple therapeutic properties of sea cucumbers with a view to exploring their potential uses as functional foods and a natural source of new multifunctional drugs.