WorldWideScience

Sample records for acid derived indices

  1. RNA:DNA ratio and other nucleic acid derived indices in marine ecology.

    Science.gov (United States)

    Chícharo, Maria A; Chícharo, Luis

    2008-08-01

    Some of most used indicators in marine ecology are nucleic acid-derived indices. They can be divided by target levels in three groups: 1) at the organism level as ecophysiologic indicators, indicators such as RNA:DNA ratios, DNA:dry weight and RNA:protein, 2) at the population level, indicators such as growth rate, starvation incidence or fisheries impact indicators, and 3) at the community level, indicators such as trophic interactions, exergy indices and prey identification. The nucleic acids derived indices, especially RNA:DNA ratio, have been applied with success as indicators of nutritional condition, well been and growth in marine organisms. They are also useful as indicators of natural or anthropogenic impacts in marine population and communities, such as upwelling or dredge fisheries, respectively. They can help in understanding important issues of marine ecology such as trophic interactions in marine environment, fish and invertebrate recruitment failure and biodiversity changes, without laborious work of counting, measuring and identification of small marine organisms. Besides the objective of integrate nucleic acid derived indices across levels of organization, the paper will also include a general characterization of most used nucleic acid derived indices in marine ecology and also advantages and limitations of them. We can conclude that using indicators, such RNA:DNA ratios and other nucleic acids derived indices concomitantly with organism and ecosystems measures of responses to climate change (distribution, abundance, activity, metabolic rate, survival) will allow for the development of more rigorous and realistic predictions of the effects of anthropogenic climate change on marine systems.

  2. Assessing the impact of environmental forcing on the condition of anchovy larvae in the Cadiz Gulf using nucleic acid and fatty acid-derived indices

    Science.gov (United States)

    Teodósio, M. A.; Garrido, S.; Peters, J.; Leitão, F.; Ré, P.; Peliz, A.; Santos, A. M. P.

    2017-02-01

    Understanding the environmental processes affecting fish larvae survival is critical for population dynamics, conservation purposes and to ecosystem-based fishery management. Using anchovies (Engraulis encrasicolus) of the Cadiz Gulf as a study case and considering the "Ocean Triad" hypothesis, we investigate the larval ecophysiological status and potential survival in relation to oceanographic variables. Therefore, this study aims to describe the nutritional condition of anchovy larvae during spawning season (peak in summer) through nucleic acid- and fatty acid (FA)-derived indices and to analyze the effects of the major environmental parameters (Depth, Temperature, Salinity, Plankton biomass) on anchovy survival potential at early phases. Fish larvae were collected in August from 30 m to 400 m depth at 35 stations off the southern Iberian coast. A previous upwelling event influenced the oceanographic conditions of the more western stations off Cape São Vicente (CSV). Along the coast, the water became warmer from west to the east through Cape Santa Maria (CSM) ending at Guadiana estuary, where easterly winds originated the development of a counter current. The standardized RNA/DNA (sRD) of anchovy larvae decreased throughout larval ontogeny, reflecting a reduction of growth during the development. Essential FA concentrations also decreased, but docosahexaenoic acid (DHA) in particular was highly conserved even after the reduction of total FA concentration in anchovy larvae related to the onset of swimming abilities (post-flexion phase). The oceanographic conditions (west upwelling, east counter current, and stratification) led to a nearshore aggregation of plankton and anchovy larvae with good ecophysiological conditions in the central area of the southern coast, where an optimal range of temperature and chlorophyll, as an indirect food proxy for anchovy larval development, were registered. The study proves that the oceanographic conditions of the study area are

  3. HPLC, TLC, and first-derivative spectrophotometry stability-indicating methods for the determination of tropisetron in the presence of its acid degradates.

    Science.gov (United States)

    Abdel-Fattah, Laila S; El-Sherif, Zeinab A; Kilani, Khadiga M; El-Haddad, Dalia A

    2010-01-01

    Three stability-indicating assay methods were developed for the determination of tropisetron in a pharmaceutical dosage form in the presence of its degradation products. The proposed techniques are HPLC, TLC, and first-derivative spectrophotometry (1D). Acid degradation was carried out, and the degradation products were separated by TLC and identified by IR, NMR, and MS techniques. The HPLC method was based on determination of tropisetron in the presence of its acid-induced degradation product on an RP Nucleosil C18 column using methanol-water-acetonitrile-trimethylamine (65 + 20 + 15 + 0.2, v/v/v/v) mobile phase and UV detection at 285 nm. The TLC method was based on the separation of tropisetron and its acid-induced degradation products, followed by densitometric measurement of the intact spot at 285 nm. The separation was carried out on silica gel 60 F254 aluminum sheets using methanol-glacial acetic acid (22 + 3, v/v) mobile phase. The 1D method was based on the measurement of first-derivative amplitudes of tropisetron in H2O at the zero-crossing point of its acid-induced degradation product at 271.9 nm. Linearity, accuracy, and precision were found to be acceptable over concentration ranges of 40-240 microg/mL, 1-10 microg/spot, and 6-36 micro/mL for the HPLC, TLC, and 1D methods, respectively. The suggested methods were successfully applied for the determination of the drug in bulk powder, laboratory-prepared mixtures, and a commercial sample.

  4. Phosphorus derivatives of salicylic acid

    Science.gov (United States)

    Chvertkina, L. V.; Khoklov, P. S.; Mironov, Vladimir F.

    1992-10-01

    The present state of work on the methods of synthesis, chemical properties, and practical applications of phosphorus-containing derivatives of salicylic acid has been reviewed. The characteristics of the chemical transformations of cyclic and acyclic phosphorus derivatives of salicylic acid related to the coordination state of the phosphorus atom have been examined. The bibliography includes 158 references.

  5. Edible Acid-Base Indicators.

    Science.gov (United States)

    Mebane, Robert C.; Rybolt, Thomas R.

    1985-01-01

    Reports on the colors observed during titrations of 15 natural indicators obtained from common fruits and vegetables. These edible indicators can be used for a variety of teacher demonstrations or for simple student experiments. (JN)

  6. Unit: Indicating Acidity, Inspection Pack, National Trial Print.

    Science.gov (United States)

    Australian Science Education Project, Toorak, Victoria.

    The introductory core activities in this trial unit, prepared for students in grades seven through nine of Australian schools, use indicators derived from flower pigments to provide a more convenient measure of acidity than taste. Students are offered choices among seven options after completion of the core: "How Acidic is That?"; "What Colour is…

  7. Study of abietic acid glycerol derivatives as microencapsulating materials.

    Science.gov (United States)

    Puranik, P K; Dorle, A K

    1991-01-01

    Abietic acid (85 per cent pure) was extracted from rosin N Grade and further standardized. Abietic acid derivatives were prepared by heating abietic acid with glycerol and intermediate reaction products with different acid values were collected. Salicylic acid granules were encapsulated using a 10 per cent solution of abietic acid and its derivatives by standard spray pan technique. The coated microcapsules were evaluated for moisture absorption, dissolution and flow properties. The result showed that abietic acid glycerol derivatives, AaG-54 and AaG-20 had better moisture protection properties. Dissolution studies indicate that these derivatives could be used for delayed release of drugs.

  8. Sedimentary environment indicators: Benzothiazole and its derivatives

    Institute of Scientific and Technical Information of China (English)

    2001-01-01

    Benzothiazoles distributional characteristics of crude oils and non-hydrocarbon fractions of source rocks in Mangya depression of the Qaidam Basin, Lunnan oil field in the Tarim Basin, Kelamayi oil field in the Junggar Basin and the Tulufan Basin oil field were analyzed. It was found that the distributions of benzothiazole are remarkable diversity in different sedimentary environmental oils. The swamp crude oils contain high quantity of benzothiazole and relatively high quantity of alkylthio-benzothiazole and 2(3H)-benzothiazolone. But the quantity of the 2,2′-dithiobis- ben-zothiazole is relatively low. The abundance of benzothiazole and 2,2′-dithiobis-benzothiazole are relatively high in semi-brackish water lacustrine crude oils, but the quantity of alkylthio-benzothiazole and 2(3H)-benzothiazolone are rela-tively low. The benzothiazoles belong to weak acid and mild base compound, and their stabilization conditions relate to their environmental medium. The nitrogenous bases are in favor of alkalescence environment, while weak acid nitroge-nous compounds are the main stable products under the weak acid environment. Benzothiazoles have great signifi-cance in identifying the oil- and gas-formed environment and the geochemistry study of non-hydrocarbon fraction in the future.

  9. The Adsorption Effect of Quaternized Chitosan Derivatives on Bile Acid

    Institute of Scientific and Technical Information of China (English)

    Shu Xian MENG; Ya Qing FENG; Wen Jin LI; Cai Xia YIN; Jin Ping DENG

    2006-01-01

    Three quaternized chitosan derivatives were synthesized and their adsorption performance of bile acid from aqueous solution was studied. The adsorption capacities and rates of bile acid onto quaternized chitosan derivatives were evaluated. The kinetic experimental data properly correlated with the second-order kinetic model, which indicated that the chemical sorption is the rate-limiting step. The results showed that the quaternized chitosan derivatives are favorable adsorbents for bile acid.

  10. The Magic Sign: Acids, Bases, and Indicators.

    Science.gov (United States)

    Phillips, Donald B.

    1986-01-01

    Presents an approach that is used to introduce elementary and junior high students to a series of activities that will provide concrete experiences with acids, bases, and indicators. Provides instructions and listings of needed solutions and materials for developing this "magic sign" device. Includes background information and several…

  11. Biological activities of substituted trichostatic acid derivatives

    Indian Academy of Sciences (India)

    Cédric Charrier; Joëlle Roche; Jean-Pierre Gesson; Philippe Bertrand

    2009-07-01

    New substituted trichostatic acid derivatives have been synthesized and evaluated for their biological activities towards the H661 non-small lung cancer cell line. These syntheses were achieved by alkylation of propiophenones to introduce the side chain with a terminal precursor of hydroxamic acid and aminobenzamide derivatives. The first fluorinated derivatives of trichostatic acid are described, such as 6-fluoro trichostatin A, with antiproliferative activities in the micromolar range and with histone deacetylase inhibitory activity.

  12. Anthranilic acid derivatives from Inula japonica

    Institute of Scientific and Technical Information of China (English)

    Jiang Jiang Qin; Hui Zi Jin; Jian Jun Fu; Xiao Jia Hu; Yan Zhu; Yun Heng Shen; Shi Kai Yan; Wei Dong Zhang

    2008-01-01

    Three new anthranilic acid derivatives, N-heneicosanoylanthranilic acid (1b), N-tricosanoylanthranilic acid (1d), N-tetra-cosanoylanthranilic acid (1e), and two known N-arachidylanthranilic acid (1a) and N-docosanoylanthranilic acid (1c) were isolatedfrom the aerial parts of Inula japonica Thunb. Their structures were established by spectroscopic and chemical methods.2008 Hui Zi Jin. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.

  13. Cholic acid derivatives: novel antimicrobials.

    Science.gov (United States)

    Savage, P B; Li, C

    2000-02-01

    Mimics of squalamine and polymyxin B (PMB) have been prepared from cholic acid in hope of finding new antimicrobial agents. The squalamine mimics include the polyamine and sulphate functionalities found in the parent antibiotic, however, the positions relative to the steroid nucleus have been exchanged. The PMB mimics include the conservation of functionality among the polymyxin family of antibiotics, the primary amine groups and a hydrophobic chain. Although the squalamine and PMB mimics are morphologically dissimilar, they display similar activities. Both are simple to prepare and demonstrate broad spectrum antimicrobial activity against Gram-negative and Gram-positive organisms. Specific examples may be inactive alone, yet effectively permeabilise the outer membranes of Gram-negative bacteria rendering them sensitive to hydrophobic antibiotics. Problems associated with some of the squalamine and PMB mimics stem from their haemolytic activity and interactions with serum proteins, however, examples exist without these side effects which can sensitise Gram-negative bacteria to hydrophobic antibiotics.

  14. Synthesis of β-Amino Acid Derivatives

    Institute of Scientific and Technical Information of China (English)

    Zhao Yonghua; Ma Zhihua; Jiang Nan; Wang Jianbo

    2004-01-01

    In recent years, β-amino acids and their derivatives have attracted considerable attention due to their occurrence in biologically active natural products, such as dolastatins,cyclohexylnorstatine and Taxol. β-Amino acids also find application in the synthesis of β-lactams,piperidines, indolizidines. Moreover, the peptides consisting of β-amino acids, the so-called β-peptides, have been extensively studied recently. Consequently, considerable efforts have been directed to the synthesis of β-amino acids and their derivatives1. In particular, stereoselective synthesis of β-amino acids has been a challenging project, and there are only limited methods available. In this presentation, we report our efforts in this area.

  15. The cytotoxic activity of ursolic acid derivatives.

    Science.gov (United States)

    Ma, Chao-Mei; Cai, Shao-Qing; Cui, Jing-Rong; Wang, Rui-Qing; Tu, Peng-Fei; Hattori, Masao; Daneshtalab, Mohsen

    2005-06-01

    Ursolic acid and 2alpha-hydroxyursolic acid isolated from apple peels were found to show growth inhibitory activity against four tumor cell lines, HL-60, BGC, Bel-7402 and Hela. Structural modifications were performed on the C-3, C-28 and C-11 positions of ursolic acid and the cytotoxicity of the derivatives was evaluated. The SAR revealed that the triterpenes possessing two hydrogen-bond forming groups (an H-donor and a carbonyl group) at positions 3 and 28 exhibit cytotoxic activity. The configuration at C-3 was found to be important for the activity. Introduction of an amino group increased the cytotoxicity greatly. A 3beta-amino derivative was 20 times more potent than the parent ursolic acid. The 28-aminoalkyl dimer compounds showed selective cytotoxicity.

  16. MODERN INDICATORS DERIVED FROM VALUE CREATION AND DISCOUNTED

    Directory of Open Access Journals (Sweden)

    Cican Simona

    2013-07-01

    In this article, we will present the connection between discounted cash flow methods and the indicators derived from value creation, based on the business finance theory, which says that firm value will increase if projects with positive net present value are accepted, while it will be destroyed if projects with negative net present value are accepted.

  17. Synthesis of isothiocyanate-derived mercapturic acids

    NARCIS (Netherlands)

    Vermeulen, M.; Zwanenburg, B.; Chittenden, G.J.F.; Verhagen, H.

    2003-01-01

    Twelve mercapturic acids derived from saturated and unsaturated aliphatic and aromatic isothiocyanates were synthesised, by adding isothiocyanate to a solution of N-acetyl-L-cysteine and sodium bicarbonate, in a typical yield of 77%. Isothiocyanates were synthesised first by adding the corresponding

  18. An Olfactory Indicator for Acid-Base Titrations.

    Science.gov (United States)

    Flair, Mark N.; Setzer, William N.

    1990-01-01

    The use of an olfactory acid-base indicator in titrations for visually impaired students is discussed. Potential olfactory indicators include eugenol, thymol, vanillin, and thiophenol. Titrations performed with each indicator with eugenol proved to be successful. (KR)

  19. Amino acid quality indices of the leaves of Clerodendrum volubile

    Directory of Open Access Journals (Sweden)

    Ochuko Lucky Erukainure

    2016-04-01

    Full Text Available Objective: To evaluate the amino acid profile and quality indices of Clerodendrum volubile (C. volubile leaves. Methods: Dried leaves of C. volubile were blended, defatted and subjected to amino acid analysis using the technicon sequential multi-sample amino acid analyzer. The amino acid quality indices which covers for chemical score, essential amino acid index, nutritional index, true digestibility, protein digestibility corrected amino acid score, and digestible indispensable amino acid score were evaluated using standard formulas. Results: Amino acid analysis revealed glutamic acid to have the highest concentration, with cysteine having the least. Aspartic acid had the highest chemical score, this was followed by glycine, histidine and arginine, respectively. The least scores were observed in serine and methionine. Glutamic acid had the highest value for true digestibility and protein digestibility corrected amino acid score, with the least observed in cysteine. Digestible indispensable amino acid score evaluation showed histidine to have the highest value for infants (birth to 6 months, threonine for children (6 months to 3 years, while isoleucine was observed to have the highest value for older children, adolescents and adults. The essential amino acid index value was less than 4, while nutritional index value was less than 0.5. Conclusions: These results indicated the leaves of C. volubile as a potential source of amino acids in the human diet as portrayed by its amino acids profile and qualities.

  20. Naturally Occurring Cinnamic Acid Sugar Ester Derivatives

    Directory of Open Access Journals (Sweden)

    Yuxin Tian

    2016-10-01

    Full Text Available Cinnamic acid sugar ester derivatives (CASEDs are a class of natural product with one or several phenylacrylic moieties linked with the non-anomeric carbon of a glycosyl skeleton part through ester bonds. Their notable anti-depressant and brains protective activities have made them a topic of great interest over the past several decades. In particular the compound 3′,6-disinapoylsucrose, the index component of Yuanzhi (a well-known Traditional Chinese Medicine or TCM, presents antidepressant effects at a molecular level, and has become a hotspot of research on new lead drug compounds. Several other similar cinnamic acid sugar ester derivatives are reported in traditional medicine as compounds to calm the nerves and display anti-depression and neuroprotective activity. Interestingly, more than one third of CASEDs are distributed in the family Polygalaceae. This overview discusses the isolation of cinnamic acid sugar ester derivatives from plants, together with a systematic discussion of their distribution, chemical structures and properties and pharmacological activities, with the hope of providing references for natural product researchers and draw attention to these interesting compounds.

  1. 21 CFR 172.862 - Oleic acid derived from tall oil fatty acids.

    Science.gov (United States)

    2010-04-01

    ... FOOD FOR HUMAN CONSUMPTION Multipurpose Additives § 172.862 Oleic acid derived from tall oil fatty acids. The food additive oleic acid derived from tall oil fatty acids may be safely used in food and as... 21 Food and Drugs 3 2010-04-01 2009-04-01 true Oleic acid derived from tall oil fatty acids....

  2. The Synthesis and Evaluation of Arctigenin Amino Acid Ester Derivatives.

    Science.gov (United States)

    Cai, En-Bo; Yang, Li-Min; Jia, Cai-Xia; Zhang, Wei-Yuan; Zhao, Yan; Li, Wei; Song, Xing-Zhuo; Zheng, Man-Ling

    2016-10-01

    The use of arctigenin (ARG), a traditional medicine with many pharmacological activities, has been restricted due to its poor solubility in water. Five amino acid derivatives of ARG have been synthesized using glycine, o-alanine, valine, leucine, and isoleucine, which have t-butyloxy carbonyl (BOC) as a protective group. In this study, we examined the effects of removing these protective groups. The results showed that the amino acid derivatives have better solubility and nitrite-clearing ability than ARG. Among the compounds tested, the amino acid derivatives without protective group were the best. Based on these results, ARG and its two amino acid derivatives without protective group (ARG8, ARG10) were selected to evaluate their anti-tumor activity in vivo at a dosage of 40 mg/kg. The results indicated that ARG8 and ARG10 both exhibit more anti-tumor activity than ARG in H22 tumor-bearing mice. The tumor inhibition rates of ARG8 and ARG10 were 69.27 and 43.58%, which was much higher than ARG. Furthermore, the mice treated with these compounds exhibited less damage to the liver, kidney and immune organs compared with the positive group. Furthermore, ARG8 and ARG10 improved the serum cytokine levels significantly compared to ARG. In brief, this study provides a method to improve the water solubility of drugs, and we also provide a reference basis for new drug development.

  3. 40 CFR 721.6097 - Phosphoric acid derivative (generic name).

    Science.gov (United States)

    2010-07-01

    ... 40 Protection of Environment 30 2010-07-01 2010-07-01 false Phosphoric acid derivative (generic... Specific Chemical Substances § 721.6097 Phosphoric acid derivative (generic name). (a) Chemical substance... phosphoric acid derivative (PMN P-95-284) is subject to reporting under this section for the significant...

  4. Bioactive Quinic Acid Derivatives from Ageratina adenophora

    Directory of Open Access Journals (Sweden)

    Jian-Wen Tan

    2013-11-01

    Full Text Available A novel quinic acid derivative, 5-O-trans-o-coumaroylquinic acid methyl ester (1, together with three known ones, chlorogenic acid methyl ester (2, macranthoin F (3 and macranthoin G (4, were isolated from the aerial parts of the invasive plant Ageratina adenophora (Spreng.. The structure of new compound 1 was elucidated on the basis of extensive spectroscopic analysis, including 1D- and 2D-NMR techniques. Compounds 2–4 were isolated from plant A. adenophora for the first time. All the compounds showed in vitro antibacterial activity toward five assayed bacterial strains, especially 3 and 4, which showed in vitro antibacterial activity against Salmonella enterica with MIC values of 7.4 and 14.7 μM, respectively. Compound 1 was further found to display in vitro anti-fungal activity against spore germination of Magnaporthe grisea with an IC50 value 542.3 µM. These four compounds were also tested for their antioxidant activity against DPPH (1,1-diphenyl-2-picrylhydrazyl radical.

  5. Quantification of acidic compounds in complex biomass-derived streams

    Energy Technology Data Exchange (ETDEWEB)

    Karp, Eric M.; Nimlos, Claire T.; Deutch, Steve; Salvachúa, Davinia; Cywar, Robin M.; Beckham, Gregg T.

    2016-01-01

    Biomass-derived streams that contain acidic compounds from the degradation of lignin and polysaccharides (e.g. black liquor, pyrolysis oil, pyrolytic lignin, etc.) are chemically complex solutions prone to instability and degradation during analysis, making quantification of compounds within them challenging. Here we present a robust analytical method to quantify acidic compounds in complex biomass-derived mixtures using ion exchange, sample reconstitution in pyridine and derivatization with BSTFA. The procedure is based on an earlier method originally reported for kraft black liquors and, in this work, is applied to identify and quantify a large slate of acidic compounds in corn stover derived alkaline pretreatment liquor (APL) as a function of pretreatment severity. Analysis of the samples is conducted with GCxGC-TOFMS to achieve good resolution of the components within the complex mixture. The results reveal the dominant low molecular weight components and their concentrations as a function of pretreatment severity. Application of this method is also demonstrated in the context of lignin conversion technologies by applying it to track the microbial conversion of an APL substrate. Here too excellent results are achieved, and the appearance and disappearance of compounds is observed in agreement with the known metabolic pathways of two bacteria, indicating the sample integrity was maintained throughout analysis. Finally, it is shown that this method applies more generally to lignin-rich materials by demonstrating its usefulness in analysis of pyrolysis oil and pyrolytic lignin.

  6. Interactions of salicylic acid derivatives with calcite crystals.

    Science.gov (United States)

    Ukrainczyk, Marko; Gredičak, Matija; Jerić, Ivanka; Kralj, Damir

    2012-01-01

    Investigation of basic interactions between the active pharmaceutical compounds and calcium carbonates is of great importance because of the possibility to use the carbonates as a mineral carrier in drug delivery systems. In this study the mode and extent of interactions of salicylic acid and its amino acid derivates, chosen as pharmaceutically relevant model compounds, with calcite crystals are described. Therefore, the crystal growth kinetics of well defined rhombohedral calcite seed crystals in the systems containing salicylic acid (SA), 5-amino salicylic acid (5-ASA), N-salicyloil-l-aspartic acid (N-Sal-Asp) or N-salicyloil-l-glutamic acid (N-Sal-Glu), were investigated. The precipitation systems were of relatively low initial supersaturation and of apparently neutral pH. The data on the crystal growth rate reductions in the presence of the applied salicylate molecules were analyzed by means of Cabrera & Vermileya's, and Kubota & Mullin's models of interactions of the dissolved additives and crystal surfaces. The crystal growth kinetic experiments were additionally supported with the appropriate electrokinetic, spectroscopic and adsorption measurements. The Langmuir adsorption constants were determined and they were found to be in a good correlation with values obtained from crystal growth kinetic analyses. The results indicated that salicylate molecules preferentially adsorb along the steps on the growing calcite surfaces. The values of average spacing between the adjacent salicylate adsorption active sites and the average distance between the neighboring adsorbed salicylate molecules were also estimated.

  7. Synthesis, antimicrobial evaluation and QSAR studies of propionic acid derivatives

    Directory of Open Access Journals (Sweden)

    Sanjiv Kumar

    2017-02-01

    Full Text Available A series of Schiff bases (1–17 and esters (18–24 of propionic acid was synthesized in appreciable yield and characterized by physicochemical as well as spectral means. The synthesized compounds were evaluated in vitro for their antimicrobial activity against Gram-positive bacteria Staphylococcus aureus, Bacillus subtilis, Gram negative bacterium Escherichia coli and fungal strains Candida albicans and Aspergillus niger by tube dilution method. Results of antimicrobial screening indicated that besides having good antibacterial activity, the synthesized compounds also displayed appreciable antifungal activity and compound 10 emerged as the most active antifungal agent (pMICca and pMICan = 1.93. The results of QSAR studies demonstrated that antibacterial, antifungal and overall antimicrobial activities of synthesized propionic acid derivatives were governed by the topological parameters, Kier’s alpha first order shape index (κα1 and valence first order molecular connectivity index (1χv.

  8. Acetylcholinesterase inhibitory properties of some benzoic acid derivatives

    Science.gov (United States)

    Yildiz, Melike; Kiliç, Deryanur; Ünver, Yaǧmur; Şentürk, Murat; Askin, Hakan; Küfrevioǧlu, Ömer Irfan

    2016-04-01

    Acetylcholinesterase (AChE) hydrolyses the neurotransmitter acetylcholine to acetic acid and choline. AChE inhibitors are used in treatment of several neurodegeneartive disorder and Alzheimer's disease. In the present study, inhibition of AChE with some benzoic acid derivatives were investigated. 3-Chloro-benzoic acid (1), 2-hydroxy-5-sulfobenzoic acid (2), 2-(sulfooxy) benzoic acid (3), 2-hydroxybenzoic acid (4), 2,3-dimethoxybenzoic (5), and 3,4,5-trimethoxybenzoic (6) were calculated IC50 values AChE enzyme. Kinetic investigations showed that similarly to AChE inhibitors. Benzoic acid derivatives (1-6) investigated are encouraging agents which may be used as lead molecules in order to derivative novel AChE inhibitors that might be useful in medical applications.

  9. Meaningful wind chill indicators derived from heat transfer principles.

    Science.gov (United States)

    Brauner, N; Shacham, M

    1995-08-01

    The wind chill index (WCI) and the more widely used wind chill equivalent temperature represent an attempt to combine several weather-related variables (temperature, wind velocity and solar radiation) into a single index which can indicate human comfort. Since its introduction in 1945, the WCI has been criticized mainly on the ground that the underlying model does not comply with modern heat transfer theory. In spite of that, the WCI, "calibrated" to human comfort, has proven to be successful in predicting discomfort and tolerance of man to the cold. Nevertheless, neither the WCI nor the wind chill equivalent temperature can be actually measured and, therefore, without the additional 'calibration' they are meaningless. In this study we have shown that the WCI represents the instantaneous rate of heat loss from bare skin at the moment of exposure to the cold, and as such, it correlates reasonably well with measurable variables that represent a feeling of cold. Two new wind chill indicators have been introduced: exposed skin temperature and maximum exposure time. These indicators yield more information than the WCI provides, are measurable, have physical meaning and are based on established heat transfer principles.

  10. Deriving vulnerability indicators for crop production regions in Indonesia

    Science.gov (United States)

    Perdinan; Atmaja, Tri; Sehabuddin, Ujang; Sugiarto, Yon; Febrianti, Lina; Farysca Adi, Ryco

    2017-01-01

    Food supply is considered as one of the most vulnerable to the effects of climate change. Higher temperature and changes in rainfall patterns and intensity may adversely impact crop production, which will eventually affect the food supply. Consequently, adaptation strategies should be devised to minimize the potential adverse impacts and maximize its potential benefits. The adaptation strategies should be devised by considering factors contributed to causing vulnerability following the concept of food supply chain, starting from production to consumption. This study focuses on identifying the contributed factors to vulnerability of crop production regions in Indonesia. The contributed factors were identified by defining indicators for each component of the food supply chain using an example of crop production centers in Indonesia, the West Java Province. The identification considers existing issues of the food supply chain, covering aspects of production, post-harvest and storage, distribution, and consumption, based on the field surveys conducted in Indramayu district of the West Java, the main grower of paddy production, and Garut district of the West Java, the main grower of corn production. The selection of the vulnerability indicators was also considered the data availability for the study area. The analysis proposed a list of indicators classified into production, post-harvest and storage, distribution and consumption that are proposed to assess the regional vulnerability of crop production regions in Indonesia. This result is expected to contribute in understanding the process of devising climate change adaptation intended for enhancing food supply resilience to climate change.

  11. Meaningful wind chill indicators derived from heat transfer principles

    Science.gov (United States)

    Brauner, Neima; Shacham, M.

    1995-03-01

    The wind chill index (WCI) and the more widely used wind chill equivalent temperature represent an attempt to combine several weather-related variables (temperature, wind velocity and solar radiation) into a single index which can indicate human comfort. Since its introduction in 1945, the WCI has been criticized mainly on the ground that the underlying model does not comply with modern heat transfer theory. In spite of that, the WCI, “calibrated” to human comfort, has proven to be successful in predicting discomfort and tolerance of man to the cold. Nevertheless, neither the WCI nor the wind chill equivalent temperature can be actually measured and, therefore, without the additional ‘calibration’ they are meaningless. In this study we have shown that the WCI represents the instantaneous rate of heat loss from bare skin at the moment of exposure to the cold, and as such, it correlates reasonably well with measurable variables that represent a feeling of cold. Two new wind chill indicators have been introduced: exposed skin temperature and maximum exposure time. These indicators yield more information than the WCI provides, are measurable, have physical meaning and are based on established heat transfer principles.

  12. Natural Cinnamic Acids, Synthetic Derivatives and Hybrids with Antimicrobial Activity

    Directory of Open Access Journals (Sweden)

    Juan David Guzman

    2014-11-01

    Full Text Available Antimicrobial natural preparations involving cinnamon, storax and propolis have been long used topically for treating infections. Cinnamic acids and related molecules are partly responsible for the therapeutic effects observed in these preparations. Most of the cinnamic acids, their esters, amides, aldehydes and alcohols, show significant growth inhibition against one or several bacterial and fungal species. Of particular interest is the potent antitubercular activity observed for some of these cinnamic derivatives, which may be amenable as future drugs for treating tuberculosis. This review intends to summarize the literature data on the antimicrobial activity of the natural cinnamic acids and related derivatives. In addition, selected hybrids between cinnamic acids and biologically active scaffolds with antimicrobial activity were also included. A comprehensive literature search was performed collating the minimum inhibitory concentration (MIC of each cinnamic acid or derivative against the reported microorganisms. The MIC data allows the relative comparison between series of molecules and the derivation of structure-activity relationships.

  13. Synthesis of azo derivatives of 4-aminosalicylic acid

    Institute of Scientific and Technical Information of China (English)

    Zheng Bao Zhao; Hui Xia Zheng; Yuan Gui Wei; Jiang Liu

    2007-01-01

    For searching a better 4-aminosalicylic acid derivative with higher activity and less side effects against the inflammatory bowel disease, 4-aminosalicylic acid (4-ASA) was protected by benzyloxycarbonyl and acetyl, respectively.The resultant was hydrogenized to remove protective group of amino group, then the product was reacted with NaNO2 to give diazonium salt, which was conjugated with salicylic acid, hydroxybenzene, N-salicyloyl glycine acid to get azo derivatives of 4-ASA.The azo derivatives were hydrolyzed under the alkaline condition to get the target products.All compounds were characterized by FT-IR, 1H NMR, 13C NMR spectra in details.New derivatives of 4-ASA were characterized.The synthetic route was reasonable and feasible.

  14. Aerosol Indices Derived from MODIS Data for Indicating Aerosol-Induced Air Pollution

    Directory of Open Access Journals (Sweden)

    Junliang He

    2014-02-01

    Full Text Available Aerosol optical depth (AOD is a critical variable in estimating aerosol concentration in the atmosphere, evaluating severity of atmospheric pollution, and studying their impact on climate. With the assistance of the 6S radiative transfer model, we simulated apparent reflectancein relation to AOD in each Moderate Resolution Imaging Spectroradiometer (MODIS waveband in this study. The closeness of the relationship was used to identify the most and least sensitive MODIS wavebands. These two bands were then used to construct three aerosol indices (difference, ratio, and normalized difference for estimating AOD quickly and effectively. The three indices were correlated, respectively, with in situ measured AOD at the Aerosol Robotic NETwork (AERONET Lake Taihu, Beijing, and Xianghe stations. It is found that apparent reflectance of the blue waveband (band 3 is the most sensitive to AOD while the mid-infrared wavelength (band 7 is the least sensitive. The difference aerosol index is the most accurate in indicating aerosol-induced atmospheric pollution with a correlation coefficient of 0.585, 0.860, 0.685, and 0.333 at the Lake Taihu station, 0.721, 0.839, 0.795, and 0.629 at the Beijing station, and 0.778, 0.782, 0.837, and 0.643 at the Xianghe station in spring, summer, autumn and winter, respectively. It is concluded that the newly proposed difference aerosol index can be used effectively to study the level of aerosol-induced air pollution from MODIS satellite imagery with relative ease.

  15. Amino acid derived 1,4-dialkyl substituted imidazolones

    DEFF Research Database (Denmark)

    Diness, Frederik; Meldal, Morten Peter

    2010-01-01

    A general method for synthesis of 1,4-substituted imidazolones from amino acids on solid support or in solution has been developed. Amino acid derived 3-Boc-(1,3)-oxazinane (Box) protected amino aldehyde building blocks were coupled through urea bonds to the amino terminal of dipeptides or amino...

  16. Caffeic Acid Derivatives in Dried Lamiaceae and Echinacea purpurea Products

    Science.gov (United States)

    The concentrations of caffeic acid derivatives within Lamiaceae and Echinacea (herb, spice, tea, and dietary supplement forms) readily available in the U.S. marketplace (n=72) were determined. After the first identification of chicoric acid in Ocimum basilicum (basil), the extent to which chicoric a...

  17. Hydrophobicity and Retention Coefficient of Selected Bile Acid Oxo Derivatives

    NARCIS (Netherlands)

    Posa, Mihalj; Pilipovic, Ana; Lalic, Mladena; Popovic, Jovan

    2010-01-01

    Retention coefficients (k) of cholic acid and its keto derivatives are determined by means of Reversed Phase High Pressure Liquid Chromatography at different temperatures (303K, 309K, and 313K). At each studied temperature, retention factor decreases if the hydroxyl group in the cholic acid molecule

  18. Injectable hydrogels derived from phosphorylated alginic acid calcium complexes

    Energy Technology Data Exchange (ETDEWEB)

    Kim, Han-Sem; Song, Minsoo, E-mail: minsoosong00@gmail.com; Lee, Eun-Jung; Shin, Ueon Sang, E-mail: usshin12@dankook.ac.kr

    2015-06-01

    Phosphorylation of sodium alginate salt (NaAlg) was carried out using H{sub 3}PO{sub 4}/P{sub 2}O{sub 5}/Et{sub 3}PO{sub 4} followed by acid–base reaction with Ca(OAc){sub 2} to give phosphorylated alginic acid calcium complexes (CaPAlg), as a water dispersible alginic acid derivative. The modified alginate derivatives including phosphorylated alginic acid (PAlg) and CaPAlg were characterized by nuclear magnetic resonance spectroscopy for {sup 1}H, and {sup 31}P nuclei, high resolution inductively coupled plasma optical emission spectroscopy, Fourier transform infrared spectroscopy, and thermogravimetric analysis. CaPAlg hydrogels were prepared simply by mixing CaPAlg solution (2 w/v%) with NaAlg solution (2 w/v%) in various ratios (2:8, 4:6, 6:4, 8:2) of volume. No additional calcium salts such as CaSO{sub 4} or CaCl{sub 2} were added externally. The gelation was completed within about 3–40 min indicating a high potential of hydrogel delivery by injection in vivo. Their mechanical properties were tested to be ≤ 6.7 kPa for compressive strength at break and about 8.4 kPa/mm for elastic modulus. SEM analysis of the CaPAlg hydrogels showed highly porous morphology with interconnected pores of width in the range of 100–800 μm. Cell culture results showed that the injectable hydrogels exhibited comparable properties to the pure alginate hydrogel in terms of cytotoxicity and 3D encapsulation of cells for a short time period. The developed injectable hydrogels showed suitable physicochemical and mechanical properties for injection in vivo, and could therefore be beneficial for the field of soft tissue engineering. - Highlights: • Preparation of water-soluble alginic acid complexes with calcium phosphate • Self-assembly of the phosphorylated alginic acid calcium complexes with sodium alginate • Preparation of injectable hydrogels with diverse gelation times within about 3–40 min.

  19. Urease inhibitory activities of beta-boswellic acid derivatives

    OpenAIRE

    Reza Hajiaghaee; Behnam Yousefi; Zinat Bahrampour Omrany; Farzaneh Nabati; Sahand Golestanian; Roya Bazl; Sanaz Golbabaei; "Shamsali Rezazadeh; Massoud Amanlou

    2013-01-01

    Background and the purpose of the study: Boswellia carterii have been used in traditional medicine for many years for management different gastrointestinal disorders. In this study, we wish to report urease inhibitory activity of four isolated compound of boswellic acid derivative.Methods 4 pentacyclic triterpenoid acids were isolated from Boswellia carterii and identified by NMR and Mass spectroscopic analysis (compounds 1, 3-O-acetyl-9,11-dehydro-beta-boswellic acid; 2, 3-O-acetyl-11-hydrox...

  20. Urease inhibitory activities of β-boswellic acid derivatives

    OpenAIRE

    Amanlou Massoud; Rezazadeh Shamsali; Hajiaghaee Reza; Nabati Farzaneh; Yousefi Behnam; Omrany Zinat Bahrampour; Golestanian Sahand; Bazl Roya; Golbabaei Sanaz

    2013-01-01

    Abstract Background and the purpose of the study Boswellia carterii have been used in traditional medicine for many years for management different gastrointestinal disorders. In this study, we wish to report urease inhibitory activity of four isolated compound of boswellic acid derivative. Methods 4 pentacyclic triterpenoid acids were isolated from Boswellia carterii and identified by NMR and Mass spectroscopic analysis (compounds 1, 3-O-acetyl-9,11-dehydro-β-boswellic acid; 2, 3-O-acetyl-11-...

  1. Syntheses,characteristics,and fluorescence properties of complexes of europium with benzoic acid and its derivatives

    Institute of Scientific and Technical Information of China (English)

    ZHOU Zhongcheng; SHU Wangen; RUAN Jianming; HUANG Boyun; LIU Younian

    2004-01-01

    The binary complexes of europium with benzoic acid and its derivatives (phthalic acid, m-phthalic acid,o-aminobenzoic acid, salicylic acid, and sulfosalicylic acid) were synthesized and their compositions were identified by elemental analyses. UV and IR of the complexes have been investigated. The UV spectra indicated that the complexes' ultraviolet absorption were mainly the ligands' absorption. The IR spectra showed that the IR spectra of complexes are different from those of free ligands. The fluorescence properties of them were investigated by using luminescence spectroscopy, the results showed that only three complexes appear as better luminescence, they were Eu-benzoic acid,Eu-m-phthalic acid and Eu-phthalic acid, while the others exhibited the ligands' wideband emission.

  2. Interaction Mechanism of Anthracene with Benzoic Acid and Its Derivatives

    Institute of Scientific and Technical Information of China (English)

    HE Ying-Ying; WANG Xiao-Chang; FAN Xiao-Yuan; ZHAO Bo; JIN Peng-Kang

    2008-01-01

    Interaction mechanism of anthracene, one of the typical polycyclic aromatic hydrocarbons, with benzoic acid and its hydroxyl-substituted derivatives, o-hydroxylbenzoic acid and p-hydroxylbenzoic acid, were studied using FFIR, UV and fluorescence spectra. The experiments confirmed that there was a specific and oriented interaction between anthracene and the aromatic carboxylic acids, and the bonding mode depended on both the chemical struc- ture of reactants and acidity of solution. The π-H hydrogen bond played a main role in the interaction between an-thracene and the aromatic carboxylic proton of benzoic acid or o-hydroxylbenzoic acid when pH≤pK, and the π-π electron donor-acceptor (EDA) interaction increasingly became the main binding mode when pH>pK. The de-crease of interaction intensity of benzoic acid was observed by introducing hydroxyl at its ortho position. The spe-cial D-π-A structure of p-hydroxylbenzoic acid made it easy to form the planar multi-molecule congeries that could interact with anthracene, so the interaction between anthracene and p-hydroxylbenzoic acid always followed the π-π EDA model no matter the solution acidity. For p-hydroxylbenzoic acid, the π-π interaction mode remained un-changed when pH increased from 2.0 to 10.0, and the binding intensity was higher than that between benzoic acid and anthracene because of the formation of the multi-molecule congeries.

  3. Oleanolic acid and related derivatives as medicinally important compounds.

    Science.gov (United States)

    Sultana, Nighat; Ata, Athar

    2008-12-01

    Oleanolic acid has been isolated from chloroform extract of Olea ferruginea Royle after removal of organic bases and free acids. The literature survey revealed it to be biologically very important. In this review the biological significance of oleanolic acid and its derivatives has been discussed. The aim of this review is to update current knowledge on oleanolic acid and its natural and semisynthetic analogs, focussing on its cytotoxic, antitumer, antioxidant, anti-inflamatory, anti-HIV, acetyl cholinesterase, alpha-glucosidase, antimicrobial, hepatoprotective, anti-inflammatory, antipruritic, spasmolytic activity, anti-angiogenic, antiallergic, antiviral and immunomodulatory activities. We present in this review, for the first time, a compilation of the most relevant scientific papers and technical reports of the chemical, pre-clinical and clinical research on the properties of oleanolic acid and its derivatives.

  4. Synthesis and mesomorphic behaviour of lithocholic acid derivatives

    Indian Academy of Sciences (India)

    V A E Shaikh; N N Maldar; S V Lonikar

    2003-08-01

    A series of liquid crystalline derivatives of lithocholic acid were prepared using simple chemical reactions involving the terminal functional group—hydroxyl at C-3 and/or carboxyl at C-24. Thus methyl -3-(3-carboxy propionyl) lithocholate (I), 3-(3-carboxy propionyl) lithocholic acid (II), 3-acetyl lithocholic acid (III), 3-propionyl lithocholic acid (IV), 3-benzoyl lithocholic acid (V), 3-(4-nitrobenzoyl) lithocholic acid (VI), 3-cinnamoyl lithocholic acid (VII), methyl-3-(4-nitrobenzoyl) lithocholate (VIII) and 1,4-bis [cholan-24-methoxy carbonyl-3-oxycarbonyl] butane (IX) were prepared in good yields and characterized by IR, NMR and polarizing optical microscopy. Compounds (I) and (IX) exhibited monotropic behaviour while the others were enantiotropic. Some of the compounds also showed a high tendency of super cooling. Compounds (V), (VI) and (IX) formed cholesteric phase while the remaining compounds displayed smectic phase.

  5. Antioxidant and cytotoxic activity of mono- and bissalicylic acid derivatives

    Directory of Open Access Journals (Sweden)

    Đurendić Evgenija A.

    2014-01-01

    Full Text Available A simple synthesis of mono- and bis-salicylic acid derivatives 1-10 by the transesterification of methyl salicylate (methyl 2-hydroxybenzoate with 3-oxapentane-1,5-diol, 3,6- dioxaoctane-1,8-diol, 3,6,9-trioxaundecane-1,11-diol, propane-1,2-diol or 1-aminopropan- 2-ol in alkaline conditions is reported. All compounds were tested in vitro on three malignant cell lines (MCF-7, MDA-MB-231, PC-3 and one non-tumor cell line (MRC- 5. Strong cytotoxicity against prostate PC-3 cancer cells expressed compounds 3, 4, 6, 9 and 10, all with the IC50 less than 10 μmol/L, which were 11-27 times higher than the cytotoxicity of antitumor drug doxorubicin. All tested compounds were not toxic against the non-tumor MRC-5 cell line. Antioxidant activity of the synthesized derivatives was also evaluated. Compounds 2, 5 and 8 were better OH radical scavengers than commercial antioxidants BHT and BHA. The synthesized compounds showed satisfactory scavenger activity, which was studied by QSAR modeling. A good correlation between the experimental variables IC50 DPPH and IC50 OH and MTI (molecular topological indices molecular descriptors and CAA (accessible Connolly solvent surface area for the new compounds 1, 3, and 5 was observed.

  6. Acidity and conductivity of Pinus massoniana bark as indicators to atmospheric acid deposition in Guangdong, China

    Institute of Scientific and Technical Information of China (English)

    KUANG Yuan-wen; ZHOU Guo-yi; WEN Da-zhi; LIU Shi-zhong

    2006-01-01

    Barks of Pinus masoniana collected from two polluted sites, Qujiang and Xiqiaoshan, and from the relatively clean site Dinghushan were used to evaluate the pollution indication by the determination of their acidity and conductivity. The acidity of the inner and outer barks from the polluted sites was significantly higher than those from the clean site, suggesting that the acidity of the bark occurred in concurrent with the air pollution. The significant lower pH values of the outer bark than the inner bark collected from all sites indicated that the outer bark was more sensitive than the inner bark in response to acid pollution, implying that the outer bark is more preferable when used as indication of atmospheric acid pollution. The conductivities of the inner barks differed significantly among the three sites, with higher values at the clean site. However, the significant differences were not observed among these sites.Furthermore, the pH values for the inner and outer barks were not correlated with the conductivity, which did not coincide with some other studies.

  7. Antibacterial and Antioxidant Activities of Ursolic Acid and Derivatives

    Directory of Open Access Journals (Sweden)

    Patrícia G.G. do Nascimento

    2014-01-01

    Full Text Available Ursolic acid, an important bioactive compound, was isolated from ethanol extract of aerial parts of Sambucus australis. In order to develop bioactive ursolic acid derivatives, two semi-synthetic compounds were obtained through modification at C-3. The antibacterial activity of the ursolic acid and its derivatives was investigated. The microdilution method was used for determination of the minimal inhibitory concentration (MIC, against twelve bacterial strains. The influence of ursolic acid and its derivatives on the susceptibility of some bacterial pathogens to the aminoglycosides antibiotics neomycin, amikacin, kanamycin and gentamicin was evaluated. The most representative synergistic effect was observed by 3β-formyloxy-urs-12-en-28-oic acid at the concentration of 64 μg/mL in combination with kanamycin against Escherichia coli (27, a multidrug-resistant clinical isolate from sputum, with reduction of MIC value from 128 μg/mL to 8 μg/mL. Ursolic acid and its derivatives were examined for their radical scavenger activity using the DPPH assay, and showed significant activity.

  8. SYNTHESIS AND PHARMACOLOGICAL SCREENING OF NSUBSTITUTED ANTHRANILIC ACID DERIVATIVES

    Directory of Open Access Journals (Sweden)

    Dileep Tiwari

    2011-06-01

    Full Text Available In the present work eight newly synthesized structurally diverse anthranilic acid derivatives were evaluated for their anti-inflammatory activity against carrageenan induced oedema in albino rats. All the anthranilic acid derivatives were compared for their percentage inhibition of the oedema using control drug phenylbutazone. The desired anthranilic acid derivatives 5-bromo-2-{[5-{[(2E-3-(2- substitutedphenylprop-2-enoyl]amino}-1,3,4,-oxadiazol-2- yl methyl]amino}benzoic acid (compounds 1-4 were synthesized by condensation of 5-bromo-N - (2'-amino acetyl -1',3',4'-oxadiazol-5'-ylmethyl anthranilic acid and substituted aromatic aldehydes, respectively, and the compounds 5-bromo-N – [2'-amino [1"-acetyl-5''- (substitutedaryl-2'-pyrazolin-3"-yl]-1'3'4'-oxadiazol-5'- ylmethyl anthranilic acid (compounds 5-8 were synthesized by the condensation of compounds (1-4 with the hydrazine hydrate in the presence of few drops of glacial acetic acid. Compound 5 was found to be a potent member of this series which showed 51.05% antiinflammatory activity with ED50 of 51.05 mg/kg while phenylbutazone exhibited 47.23% anti-inflammatory activity at the same dose. The structures of the newly synthesized compounds have been established on the basis of spectral (FTIR and 1H-NMR data and elemental analysis.

  9. Effect of cholic acid and its keto derivatives on the analgesic action of lidocaine and associated biochemical parameters in rats.

    Science.gov (United States)

    Posa, Mihalj; Kevresan, Slavko; Mikov, Momir; Cirin-Novta, Vera; Kuhajda, Ksenija

    2007-01-01

    This study examined the effect of the structure and concentration of cholic acid and its keto derivatives on the local analgesic action of lidocaine in rats, measured by an analgesimetric method. The increase in bile acid concentrations in the administered lidocaine solution increased the duration of local anesthesia. It was found that the introduction of keto groups into the cholic acid molecule yielded derivatives with lower promotory action, i.e. decreased the duration of local anesthesia. The biochemical parameters investigated indicated that the keto derivatives of cholic acid exhibited no toxicity compared to that of cholic acid itself.

  10. Pyromeconic acid derivatives from Conyza canadnsis (L.) Cronq

    Institute of Scientific and Technical Information of China (English)

    Bai Lian Liu; Guo Cai Wang; Hong Li Liu; Yi Dai; Wen Cai Ye; Yao Lan Li

    2011-01-01

    A new pyromeconic acid derivative, pyromeconic acid-3-O-β-D-glucopyranoside-3'-(O-β-D-glucopyranoside)-6'-(O-4"-hydro-xybenzoate) (1), along with two known ones, were isolated from the whole plants of Conyza canadensis. Their structures were elucidated based on the analysis of their spectroscopic data. The in vitro antibacterial testing results showed that all of these three compounds were inactive towards two bacterial strains, Escherichia coli and Staphyloccocus aureus.

  11. A New Ph Indicator Based on 2,5-Diaryl-1-salicylideneamino-1, 3, 4-triazole Derivative

    Institute of Scientific and Technical Information of China (English)

    GUNDOGDU,Ali; BULUT,Volkan,N.; DURAN,Celal; KEMER,Baris; BEKIRCAN,Olcay; SOYLAK,Mustafa

    2008-01-01

    2-Phenyl-5-p-tolyl-1-salicylideneamino-1,3,4-triazole (PTST) was studied among 2,5-diaryl-1-salicylidene amino-1,3,4-triazole derivatives as a novel potential pH indicator. In terms of absorption intensity coming from the acid-base reactions, PTST showed strong yellow-green colour with high extinction coefficient in the pH range 7.0-9.5. In addition, the corresponding colour development at the transition point can be attributed to the resonance structures of PTST, which were caused by the hydrogen ion dissociation from the acidic form of the compound in the presence of alkali. The full geometric optimization and achievement of the electronic structure of the molecule were performed by an AM1 semiempirical method. The triazole compound was compared with phenolphthalein (PT), which is widely used as an acid-base indicator in titrimetry, for accuracy test.

  12. Nutritional value of D-amino acids, D-peptides, and amino acid derivatives in mice.

    Science.gov (United States)

    Friedman, Mendel; Levin, Carol E

    2012-01-01

    This paper describes a method for determining the nutritional value of D-amino acids, D-peptides, and amino acid derivatives using a growth assay in mice fed a synthetic all-amino acid diet. A large number of experiments were carried out in which a molar equivalent of the test compound replaced a nutritionally essential amino acid such as L-lysine (L-Lys), L-methionine (L-Met), L -phenylalanine (L-Phe), and L-tryptophan (L-Trp) as well as the semi-essential amino acids L-cysteine (L-Cys) and L-tyrosine (L-Tyr). The results show wide-ranging variations in the biological utilization of test substances. The method is generally applicable to the determination of the biological utilization and safety of any amino acid derivative as a potential nutritional source of the corresponding L-amino acid. Because the organism is forced to use the D-amino acid or amino acid derivative as the sole source of the essential or semi-essential amino acid being replaced, and because a free amino acid diet allows better control of composition, the use of all-amino acid for such determinations may be preferable to protein-based diets.

  13. An Alternative to Synthetic Acid Base Indicator-Tagetes Erecta Linn

    Directory of Open Access Journals (Sweden)

    *A. Elumalai

    2012-06-01

    Full Text Available The present work highlights the use of the methanolic extract of the flowers of Tagetes erecta as an acid-base indicator in acid-base titrations. This natural indicator is easy to extract as well as easily available. Indicators used in titration show well marked changes of colour in certain intervals of pH. Most of these indicators are organic dyes and are of synthetic origin. Today synthetic indicators are the choice of acid-base titrations. But due to environmental pollution, availability and cost, the search for natural compounds as an acid-base indicator was started. Herbal indicators are evaluated by using strong acid-strong base, strong acid-weak base, weak acid-strong base and weak acid weak base. In all these titrations the methanolic extract of the flowers of Tagetes erecta was found to be very useful, economical, simple and accurate for acid base titration.

  14. Synthesis of ellagic acid and its 4,4'-di-Ο-alky derivatives from gallic acid

    OpenAIRE

    Alam, Ashraful; 高口, 豊; 坪井, 貞夫

    2005-01-01

    Synthesis of ellagic acid and its 4,4'-di-Ο-alkyl derivatives from gallic acid is described. Ellagic acid is prepared by oxidative coupling of gallic acid with ο-chloranil. Functionalized methyl bormogallate underwent Ullmann coupling to give the biphenyl that upon lactonization resulted in the ellagic acid and its alkoxy derivatives.

  15. Anti-Trichomonas vaginalis activity of betulinic acid derivatives.

    Science.gov (United States)

    Hübner, Dariana Pimentel Gomes; de Brum Vieira, Patrícia; Frasson, Amanda Piccoli; Menezes, Camila Braz; Senger, Franciane Rios; Santos da Silva, Gloria Narjara; Baggio Gnoatto, Simone Cristina; Tasca, Tiana

    2016-12-01

    Caused by Trichomonas vaginalis, trichomoniasis is the most common non-viral STD worldwide. Currently, metronidazole and tinidazole are the only drugs approved for treatment of the condition. However, problems such as metronidazole-resistant T. vaginalis isolates and allergic reactions have been reported. Based on data previously published by our group, structural changes in betulinic acid (1) were performed, generating three new compounds that were tested for in vitro anti-T.vaginalis activity in this study. Whereas derivative 2 did not demonstrate anti-T. vaginalis activity, derivatives 3 and 4 reduced trophozoite viability by 100%, with MIC values of 50μM. The structural difference of two compounds was performed only on the C-28 position. Derivative 3 showed low cytotoxicity against Vero cells in 24h; however, derivative 4 was highly cytotoxic, but efficient when associated with metronidazole in the synergism assay. ROS production by neutrophils was reduced, and derivative 3 showed anti-inflammatory effect. Collectively, the results of this study provide in vitro evidence that betulinic acid derivatives 3 and 4 are potential compounds with anti-T. vaginalis activity.

  16. Synthesis of new hyodeoxycholic acid thiosemicarbazone derivatives under solvent-free conditions using microwave

    Institute of Scientific and Technical Information of China (English)

    Zhi Chuan Shi; Zhi Gang Zhao; Xing Li Liu; Yu Chen

    2011-01-01

    An efficient and simple method for synthesis of new hyodeoxycholic acid thiosemicarbazone derivatives under solvent-free conditions using microwave has been developed. Its main advantages are short reaction times, good conversions and the environmentally friendly nature of the process. The preliminary results indicate that some of these compounds possess inhibitory effects against E. coli.

  17. Zoledronic acid in the treatment of osteoporosis: indications for use

    Directory of Open Access Journals (Sweden)

    Nataliya Vladimirovna Toroptsova

    2011-06-01

    Full Text Available The mechanism of action of the third-generation bisphosphonate zoledronic acid (Aclasta is described; the data of randomized clinical trials of its efficacy and tolerability are given. It is concluded that zoledronic acid intravenously administered once a year may be the drug of choice for increasing patients' adherence to therapy, particularly in polypharmacy that is common in the elderly and in cognitive disorders. In addition, the drug may be given to postmenopausal women once every 2 years for the prevention of osteoporosis.

  18. Caldensinic acid, a benzoic acid derivative and others compounds from Piper carniconnectivum

    Energy Technology Data Exchange (ETDEWEB)

    Alves, Harley da Silva; Souza, Maria de Fatima Vanderlei de; Chaves, Maria Celia de Oliveira, E-mail: cchaves@ltf.ufpb.b [Universidade Federal da Paraiba (UFPB), Joao Pessoa, PB (Brazil). Lab. de Tecnologia Farmaceutica

    2010-07-01

    A benzoic acid derivative - caldensinic acid, E-phythyl hexadecanoate, {beta}-sitosterol and stigmasterol mixture and phaeophytin a were isolated from the aerial parts of Piper carniconnectivum. The structures of these compounds were established unambiguously by IR, MS, 1D and 2D NMR analysis. (author)

  19. Derivative vegetation indices as a new approach in remote sensing of vegetation

    Institute of Scientific and Technical Information of China (English)

    Svetlana M.KOCHUBEY; Taras A.KAZANTSEV

    2012-01-01

    This paper focuses on the advantages of derivative vegetation indices over simple reflectancebased indices that are traditionally used for remote sensing of vegetation.The idea of using reflectance derivatives instead of simple reflectance spectra was proposed several decades ago.Despite this,it has not been widely used in monitoring systems because the derivatives lack reliable parameters.In addition,most satellite monitoring systems are not equipped with hyperspectral sensors,which are considered necessary for operating with the reflectance derivatives.Here,we present original data indicating that the chlorophyll-related derivative index D725/D702 we derived can be accurately estimated from a reflectance spectrum of 10 nm resolution that would be suitable for most satellite-based sensors.Furthermore,the index is not sensitive to soil reflectance and can therefore be used for testing of open crops.Presence of blanc reflectance is also unnecessary.Preliminary results of index testing are presented.Perspectives on using this and other derivative indices are discussed.

  20. Carboxylic Acids as Indicators of Parent Body Conditions

    Science.gov (United States)

    Lerner N. R.; Chang, Sherwood (Technical Monitor)

    1995-01-01

    Alpha-hydroxy and alpha-amino carboxylic acids found on the Murchison meteorite are deuterium enriched. It is postulated that they arose from a common interstellar scurce: the reaction of carbonyl compounds in an aqueous mixture containing HCN and NH3. Carbonyl compounds react with HCN to form alpha-hydroxy nitriles, RR'CO + HCN right and left arrow RR'C(OH)CN. If ammonia is also present, the alpha-hydroxy nitriles will exist in equilibrium with the alpha-amino nitriles, RR'C(OH)CN + NH3 right and left arrow - RRCNH2CN + H2O. Both nitrites are hydrolyzed by water to form carboxylic acids: RR'C(OH)CN + H2O yields RR'C(OH)CO2H and RR'C(NH2)CN + H2O yields RR'C(NH2)CO2H.

  1. Biological Activities of Oleanolic Acid Derivatives from Calendula officinalis Seeds.

    Science.gov (United States)

    Zaki, Ahmed; Ashour, Ahmed; Mira, Amira; Kishikawa, Asuka; Nakagawa, Toshinori; Zhu, Qinchang; Shimizu, Kuniyoshi

    2016-05-01

    Phytochemical examination of butanol fraction of Calendula officinalis seeds led to the isolation of two compounds identified as 28-O-β-D-glucopyranosyl-oleanolic acid 3-O-β-D-glucopyranosyl (1→3)-β-D-glucopyranosiduronic acid (CS1) and oleanolic acid 3-O-β-D-glucopyranosyl (1→3)-β-D-glucopyranosiduronic acid (CS2). Biological evaluation was carried out for these two compounds such as melanin biosynthesis inhibitory, hyaluronic acid production activities, anti obesity using lipase inhibition and adipocyte differentiation as well as evaluation of the protective effect against hydrogen peroxide induced neurotoxicity in neuro-2A cells. The results showed that, compound CS2 has a melanin biosynthesis stimulatory activity; however, compound CS1 has a potent stimulatory effect for the production of hyaluronic acid on normal human dermal fibroblast from adult (NHDF-Ad). Both compounds did not show any inhibitory effect on both lipase and adipocyte differentiation. Compound CS2 could protect neuro-2A cells and increased cell viability against H2 O2 . These activities (melanin biosynthesis stimulatory and protective effect against H2 O2 of CS2 and hyaluronic acid productive activities of these triterpene derivatives) have been reported for the first time. Copyright © 2016 John Wiley & Sons, Ltd.

  2. An elementary derivation of the hard/soft-acid/base principle.

    Science.gov (United States)

    Ayers, Paul W

    2005-04-08

    The hard/soft-acid/base (HSAB) principle indicates that hard acids prefer binding to hard bases (often forming bonds with substantial ionic character) while soft acids prefer binding to soft bases (often forming bonds with substantial covalent character). Though the HSAB principle is a foundational concept of the modern theory of acids and bases, the theoretical underpinnings of the HSAB principle remain murky. This paper examines the exchange reaction, wherein two molecules, one the product of reacting a hard acid and a soft base and the other the product of reacting a soft acid with a hard base, exchange substituents to form the preferred hard-hard and soft-soft product. A simple derivation shows that this reaction is exothermic, proving the validity of the HSAB principle. The analysis leads to the simple and conceptually appealing conclusion that the HSAB principle is a driven by simple electron transfer effects.

  3. Opuntia ficus indica (L.) Fruit Extract as Natural Indicator in Acid-Base Titration

    OpenAIRE

    Manoj A. Suva

    2014-01-01

    In routine experiments synthetic indicators are the choice of acid base titrations. But there are some limitations like environmental pollution, availability and higher cost which leads to search for natural compounds as an acid base indicator was started. The present work highlights theexploit of the methanolic and aqueous extract of the fruit of Opuntia ficus indica plants as a natural acid base indicator in acid base titrations. Opuntia ficus indica plant was identified and fruits were was...

  4. Preparation and adsorption behavior for metal ions and humic acid of chitosan derivatives crosslinked by irradiation

    Institute of Scientific and Technical Information of China (English)

    2007-01-01

    This article deals with the determination of the adsorption properties of metal ions and humic acid in water on crosslinked chitosan derivatives (carboxymethylchitosan) which were formed using the irradiation technique without any additives. The solubility test of these crosslinked materials were investigated in acidic, alkaline media,distilled water, and certain organic solvents. Scanning electron microscopic (SEM) images showed that the crosslinked chitosan derivatives possessed a porous morphological structure. Charged characteristic analyses demonstrated typically pH-dependent properties of the crosslinked materials. The adsorption studies were carried out by the batch method at room temperature. Adsorption of heavy metal ions (such as Cu2+, Cd2+) and humic acid onto crosslinked samples was found to be strongly pH-dependent. Adsorption kinetic studies indicated the rapid removal of metal ions, and humic acid from the aqueous solutions. Moreover, isothermal adsorption data revealed that Cu2+, Cd2+,and humic acid were removed by these crosslinked materials with high efficiency. Adsorption isothermal data were interpreted well by the Langmuir equation. These crosslinked carboxymethylated chitosan derivatives indicate favorable adsorption of metal ions and humic acid.

  5. Food group diversity indicators derived from qualitative list-based questionnaire misreported some foods compared to same indicators derived from quantitative 24-hour recall in urban Burkina Faso.

    Science.gov (United States)

    Martin-Prevel, Yves; Becquey, Elodie; Arimond, Mary

    2010-11-01

    To be useful proxies of micronutrient intake at the population level in resource-limited societies, dietary diversity indicators should be simple and easy to collect in large surveys and their accuracy needs to be assessed. The present study aimed at comparing food group diversity indicators (FGI) derived from simple qualitative list-based questionnaires (qFGI) to the same indicators derived from quantitative 24-h recalls (QFGI). Both methods were administered separately on each of 3 recall days to women in 2 districts of Ouagadougou, Burkina Faso. Data were available for a total of 526 women x recalls. This study was performed within the framework of the Women's Dietary Diversity Project, which sought to analyze the relationships between various QFGI and the mean probability of adequacy (MPA) of women's diets across 11 micronutrients. The comparison between paired qFGI and QFGI scores was made both in terms of accuracy of the reporting by the list-based questionnaire, taking the QFGI as the gold standard, and in terms of performance of indicators in predicting an MPA > 60%. Examination of paired QFGI-qFGI differences revealed that the more disaggregated the FGI, the higher were the mean differences in scores. Food groups most frequently misreported often corresponded to foods put in small quantities in sauces. Overreporting by list-based questionnaires was observed for indicators applying a 15-g minimum quantity of consumption for a group to count in the score and this may result in weaker performance in predicting the MPA. These results highlight trade-offs between accuracy and simplicity when operationalizing FGI through qualitative questionnaires.

  6. Weakening of salmonella with selected microbial metabolites of berry-derived phenolic compounds and organic acids.

    Science.gov (United States)

    Alakomi, Hanna-Leena; Puupponen-Pimiä, Riitta; Aura, Anna-Marja; Helander, Ilkka M; Nohynek, Liisa; Oksman-Caldentey, Kirsi-Marja; Saarela, Maria

    2007-05-16

    Gram-negative bacteria are important food spoilage and pathogenic bacteria. Their unique outer membrane (OM) provides them with a hydrophilic surface structure, which makes them inherently resistant to many antimicrobial agents, thus hindering their control. However, with permeabilizers, compounds that disintegrate and weaken the OM, Gram-negative cells can be sensitized to several external agents. Although antimicrobial activity of plant-derived phenolic compounds has been widely reported, their mechanisms of action have not yet been well demonstrated. The aim of our study was to elucidate the role of selected colonic microbial metabolites of berry-derived phenolic compounds in the weakening of the Gram-negative OM. The effect of the agents on the OM permeability of Salmonella was studied utilizing a fluorescence probe uptake assay, sensitization to hydrophobic antibiotics, and lipopolysaccharide (LPS) release. Our results show that 3,4-dihydroxyphenylacetic acid, 3-hydroxyphenylacetic acid, 3-(3,4-dihydroxyphenyl)propionic acid (3,4-diHPP), 3-(4-hydroxyphenyl)propionic acid, 3-phenylpropionic acid, and 3-(3-hydroxyphenyl)propionic acid efficiently destabilized the OM of Salmonella enterica subsp. enterica serovar Typhimurium and S. enterica subsp. enterica serovar Infantis as indicated by an increase in the uptake of the fluorescent probe 1-N-phenylnaphthylamine (NPN). The OM-destabilizing activity of the compounds was partially abolished by MgCl2 addition, indicating that part of their activity is based on removal of OM-stabilizing divalent cations. Furthermore, 3,4-dihydroxyphenylacetic acid, 3-hydroxyphenylacetic acid, and 3,4-diHPP increased the susceptibility of S. enterica subsp. enterica serovar Typhimurium strains for novobiocin. In addition, organic acids present in berries, such as malic acid, sorbic acid, and benzoic acid, were shown to be efficient permeabilizers of Salmonella as shown by an increase in the NPN uptake assay and by LPS release.

  7. Anacardic acid derivatives from Brazilian propolis and their antibacterial activity

    Energy Technology Data Exchange (ETDEWEB)

    Silva, M.S.S.; Lima, S.G. de; Lopes, J.A.D.; Chaves, M.H.; Cito, A.M.G.L. [Universidade Federal do Piaui (UFPI), Teresina, PI (Brazil). Dept. de Quimica]. E-mail: gracito@ufpi.br; Oliveira, E.H. [Universidade Federal do Piaui (UFPI), Teresina, PI (Brazil). Dept. de Microbiologia e Parasitologia; Reis, F.A.M. [Universidade Estadual de Campinas (UNICAMP), Campinas, SP (Brazil). Inst. de Quimica

    2008-07-01

    Propolis is a sticky, gummy, resinous substance collected by honeybees (Apis mellifera L.) from various plant sources, which has excellent medicinal properties. This paper describes the isolation and identification of triterpenoids and anacardic acid derivatives from Brazilian propolis and their antibacterial activity. Their structures were elucidated by {sup 1}H and {sup 13}C NMR, including uni- and bidimensional techniques; in addition, comparisons were made with data from academic literature. These compounds were identified as: cardanols (1a + 1b), cardols (2a + 2b), mono ene anacardic acid (3), alpha-amirine (4), beta-amirine (5), cycloartenol (6), 24-methylene-cycloartenol (7) and lupeol (8). The determination of the position of the double bond after a reaction with Dimethyl disulfide (DMDS) is described for the phenol derivatives. The ethanolic extract was tested in vitro for antimicrobial activity by using the disc diffusion method and it showed significant results against Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa and Shigella spp. (author)

  8. Neuraminidase inhibition of Dietary chlorogenic acids and derivatives - potential antivirals from dietary sources.

    Science.gov (United States)

    Gamaleldin Elsadig Karar, Mohamed; Matei, Marius-Febi; Jaiswal, Rakesh; Illenberger, Susanne; Kuhnert, Nikolai

    2016-04-01

    Plants rich in chlorogenic acids (CGAs), caffeic acids and their derivatives have been found to exert antiviral effects against influenza virus neuroaminidase. In this study several dietary naturally occurring chlorogenic acids, phenolic acids and derivatives were screened for their inhibitory activity against neuroaminidases (NAs) from C. perfringens, H5N1 and recombinant H5N1 (N-His)-Tag using a fluorometric assay. There was no significant difference in inhibition between the different NA enzymes. The enzyme inhibition results indicated that chlorogenic acids and selected derivatives, exhibited high activities against NAs. It seems that the catechol group from caffeic acid was important for the activity. Dietary CGA therefore show promise as potential antiviral agents. However, caffeoyl quinic acids show low bioavailibility and are intensly metabolized by the gut micro flora, only low nM concentrations are observed in plasma and urine, therefore a systemic antiviral effect of these compounds is unlikely. Nevertheless, gut floral metabolites with a catechol moiety or structurally related dietary phenolics with a catechol moiety might serve as interesting compounds for future investigations.

  9. Ionic derivatives of betulinic acid as novel HIV-1 protease inhibitors.

    Science.gov (United States)

    Zhao, Hua; Holmes, Shaletha S; Baker, Gary A; Challa, Suresh; Bose, Himangshu S; Song, Zhiyan

    2012-10-01

    Betulinic acid is a natural product possessing abundant and favourable biological activity, including anti-cancer, anti-malarial, anti-inflammatory and anti-HIV properties, while causing minimal toxicity to unaffected cells. The full biological potency of betulinic acid cannot be fully unlocked, however, for a number of reasons, a primary one being its limited solubility in aqueous and biologically pertinent organic media. Aiming to improve the water solubility of betulinic acid without disrupting its structurally related bioactivity, we have prepared different ionic derivatives of betulinic acid. Inhibition bioassays on HIV-1 protease-catalysed peptide hydrolysis indicate significantly improved performance resulting from converting the betulinic acid to organic salt form. Indeed, for one particular cholinium-based derivative, its water solubility is improved more than 100 times and the half maximal inhibitory concentration (IC(50)) value (22 μg mL(-1)) was one-third that of wide-type betulinic acid (60 μg mL(-1)). These encouraging results advise that additional studies of ionic betulinic acid derivatives as a therapeutic solution against HIV-1 infection are warranted.

  10. Urease inhibitory activities of beta-boswellic acid derivatives

    Directory of Open Access Journals (Sweden)

    Reza Hajiaghaee

    2013-01-01

    Full Text Available Background and the purpose of the study: Boswellia carterii have been used in traditional medicine for many years for management different gastrointestinal disorders. In this study, we wish to report urease inhibitory activity of four isolated compound of boswellic acid derivative.Methods 4 pentacyclic triterpenoid acids were isolated from Boswellia carterii and identified by NMR and Mass spectroscopic analysis (compounds 1, 3-O-acetyl-9,11-dehydro-beta-boswellic acid; 2, 3-O-acetyl-11-hydroxy-beta-boswellic acid; 3. 3-O- acetyl-11-keto-beta-boswellic acid and 4, 11-keto-beta-boswellic acid. Their inhibitory activity on Jack bean urease were evaluated. Docking and pharmacophore analysis using AutoDock 4.2 and Ligandscout 3.03 programs were also performed to explain possible mechanism of interaction between isolated compounds and urease enzyme.Results It was found that compound 1 has the strongest inhibitory activity against Jack bean urease (IC50 = 6.27 +/- 0.03 muM, compared with thiourea as a standard inhibitor (IC50 = 21.1 +/- 0.3 muM.Conclusion The inhibition potency is probably due to the formation of appropriate hydrogen bonds and hydrophobic interactions between the investigated compounds and urease enzyme active site and confirms its traditional usage.

  11. Urease inhibitory activities of β-boswellic acid derivatives

    Directory of Open Access Journals (Sweden)

    Amanlou Massoud

    2013-01-01

    Full Text Available Abstract Background and the purpose of the study Boswellia carterii have been used in traditional medicine for many years for management different gastrointestinal disorders. In this study, we wish to report urease inhibitory activity of four isolated compound of boswellic acid derivative. Methods 4 pentacyclic triterpenoid acids were isolated from Boswellia carterii and identified by NMR and Mass spectroscopic analysis (compounds 1, 3-O-acetyl-9,11-dehydro-β-boswellic acid; 2, 3-O-acetyl-11-hydroxy-β-boswellic acid; 3. 3-O- acetyl-11-keto-β-boswellic acid and 4, 11-keto-β-boswellic acid. Their inhibitory activity on Jack bean urease were evaluated. Docking and pharmacophore analysis using AutoDock 4.2 and Ligandscout 3.03 programs were also performed to explain possible mechanism of interaction between isolated compounds and urease enzyme. Results It was found that compound 1 has the strongest inhibitory activity against Jack bean urease (IC50 = 6.27 ± 0.03 μM, compared with thiourea as a standard inhibitor (IC50 = 21.1 ± 0.3 μM. Conclusion The inhibition potency is probably due to the formation of appropriate hydrogen bonds and hydrophobic interactions between the investigated compounds and urease enzyme active site and confirms its traditional usage.

  12. 76 FR 11891 - Temperature-Indicating Devices; Thermally Processed Low-Acid Foods Packaged in Hermetically...

    Science.gov (United States)

    2011-03-03

    ... 113 Temperature-Indicating Devices; Thermally Processed Low-Acid Foods Packaged in Hermetically Sealed... Temperature-Indicating Devices; Thermally Processed Low-Acid Foods Packaged in Hermetically Sealed Containers... (FDA) is amending its regulations for thermally processed low-acid foods packaged in...

  13. Starch Modification by Organic Acids and Their Derivatives: A Review

    Directory of Open Access Journals (Sweden)

    Đurđica Ačkar

    2015-10-01

    Full Text Available Starch has been an inexhaustible subject of research for many decades. It is an inexpensive, readily-available material with extensive application in the food and processing industry. Researchers are continually trying to improve its properties by different modification procedures and expand its application. What is mostly applied in this view are their chemical modifications, among which organic acids have recently drawn the greatest attention, particularly with respect to the application of starch in the food industry. Namely, organic acids naturally occur in many edible plants and many of them are generally recognized as safe (GRAS, which make them ideal modification agents for starch intended for the food industry. The aim of this review is to give a short literature overview of the progress made in the research of starch esterification, etherification, cross-linking, and dual modification with organic acids and their derivatives.

  14. Evaluation of antioxidant properties of monoaromatic derivatives of pulvinic acids.

    Science.gov (United States)

    Habrant, Damien; Poigny, Stéphane; Ségur-Derai, Muriel; Brunel, Yves; Heurtaux, Benoît; Le Gall, Thierry; Strehle, Axelle; Saladin, Régis; Meunier, Stéphane; Mioskowski, Charles; Wagner, Alain

    2009-04-23

    The natural mushroom pigment Norbadione A and three other pulvinic acids were shown by our group to display very efficient antioxidant properties by comparison with a collection of potent molecules including catechols, flavonoids, stilbenes, or coumarins. Despite numerous publications on robust and straightforward synthetic access to pulvinic acids by us and others, no report has been made to unravel the structure-activity relationships that govern the striking antioxidant activity. Herein is presented the synthesis of 18 diverse pulvinic acid derivatives and the study of their radical scavenging capacities by four different assays. The influence of each of the two phenyl rings, of their substituents and of the lateral chain on the antioxidant properties, was explored to reveal a simplified structure of excellent activity. These results, along with the absence of cytotoxicity, make the synthesized compounds interesting to evaluate for several biological activities and especially for anti-inflammatory effects and skin protection against UV induced oxidative stress.

  15. The Effects of Malonic Acid Derivatives and Acetic Acid Derivatives as Coadsorbents on the Photovoltaic Performance of Dye-Sensitized Solar Cells

    Directory of Open Access Journals (Sweden)

    Hiroaki Matsuyoshi

    2013-01-01

    Full Text Available The effects of malonic acid derivatives and acetic acid derivatives as coadsorbents on the photovoltaic performance of D908 dye-sensitized nanocrystalline TiO2 solar cells were investigated. Each of phenylmalonic acid (PMA and cyclopentylacetic acid (CPEAA coadsorptions was revealed to improve both the photocurrent and the photovoltage of the solar cells. The improved photocurrent was probably due to the suppression of self-quenching of the excited electrons in the dyes by coadsorption of PMA or CPEAA on the TiO2 that increased in the electron-injection yields from the dye to the TiO2. The improved photovoltage was probably due to suppression of recombination between the injected electrons and ions on the TiO2 surface. ATR-FTIR spectroscopy indicated that PMA or CPEAA coadsorption increased the content of bound dye on the TiO2 surface. This result suggests that PMA or CPEAA coadsorption improved the photocurrent of the solar cells. Electrochemical impedance spectroscopy indicated that PMA or CPEAA coadsorption on the TiO2 surface increased the charge recombination resistance (R2 and decreased the diffusion resistance in the electrolyte (R3. These results suggest that the coadsorption of PMA or CPEAA on the TiO2 may improve its photovoltage and photocurrent.

  16. Comparison of rainfall based SPI drought indices with SMDI and ETDI indices derived from a soil water budget model

    Science.gov (United States)

    Houcine, A.; Bargaoui, Z.

    2012-04-01

    Modelling soil water budget is a key issue for assessing drought awareness indices based on soil moisture estimation. The aim of the study is to compare drought indices based on rainfall time series to those based on soil water content time series and evapotranspiration time series. To this end, a vertically averaged water budget over the root zone is implemented to assist the estimation of evapotranspiration flux. A daily time step is adopted to run the water budget model for a lumped watershed of 250 km2 under arid climate where recorded meteorological and hydrological data are available for a ten year period. The water balance including 7 parameters is computed including evapotranspiration, runoff and leakage. Soil properties related parameters are derived according to pedo transfer functions while two remaining parameters are considered as data driven and are subject to calibration. The model is calibrated using daily hydro meteorological data (solar radiation, air temperature, air humidity, mean areal rainfall) as well as daily runoff records and also average annual (or regional) evapotranspiration. The latter is estimated using an empirical sub-model. A set of acceptable solutions is identified according to the values of the Nash coefficients for annual and decadal runoffs as well as the relative bias for average annual evapotranspiration. Using these acceptable solutions several drought indices are computed: SPI (standard precipitation index), SMDI (soil moisture deficit index) and ETDI (evapotranspiration deficit index). While SPI indicators are based only on monthly precipitation time series, SMDI are based on weekly mean soil water content as computed by the hydrological model. On the other hand ETDI indices are based on weekly mean potential and actual evapotranspirations as estimated by the meteorological and hydrological models. For SPI evaluation various time scales are considered from one to twelve months (SPI1, SPI3, SPI6, SPI9 and SPI12). For all

  17. Amino acid quality indices of the leaves ofClerodendrum volubile

    Institute of Scientific and Technical Information of China (English)

    Ochuko Lucky Erukainure; Folashade Oluwayemisi Owolabi; Temiloluwa Adebola Adesioye; Deborah Olabisi Akinyele; Grace Ijeoma Okonrokwo

    2016-01-01

    Objective: To evaluate the amino acid profile and quality indices ofClerodendrumvolubile (C. volubile) leaves. Methods:Dried leaves ofC. volubile were blended, defatted and subjected to amino acid analysis using the technicon sequential multi-sample amino acid analyzer. The amino acid quality indices which covers for chemical score, essential amino acid index, nutritional index, true digestibility, protein digestibility corrected amino acid score, and digestible indispensable amino acid score were evaluated using standard formulas. Results: Amino acid analysis revealed glutamic acid to have the highest concentration, with cysteine having the least. Aspartic acid had the highest chemical score, this was followed by glycine, histidine and arginine, respectively. The least scores were observed in serine and methionine. Glutamic acid had the highest value for true digestibility and protein digestibility corrected amino acid score, with the least observed in cysteine. Digestible indispensable amino acid score evaluation showed histidine to have the highest value for infants (birth to 6 months), threonine for children (6 months to 3 years), while isoleucine was observed to have the highest value for older children, adolescents and adults. The essential amino acid index value was less than 4, while nutritional index value was less than 0.5. Conclusions:These results indicated the leaves ofC. volubile as a potential source of amino acids in the human diet as portrayed by its amino acids profile and qualities.

  18. Nitrogenous compounds stimulate glucose-derived acid production by oral Streptococcus and Actinomyces.

    Science.gov (United States)

    Norimatsu, Yuka; Kawashima, Junko; Takano-Yamamoto, Teruko; Takahashi, Nobuhiro

    2015-09-01

    Both Streptococcus and Actinomyces can produce acids from dietary sugars and are frequently found in caries lesions. In the oral cavity, nitrogenous compounds, such as peptides and amino acids, are provided continuously by saliva and crevicular gingival fluid. Given that these bacteria can also utilize nitrogen compounds for their growth, it was hypothesized that nitrogenous compounds may influence their acid production; however, no previous studies have examined this topic. Therefore, the present study aimed to assess the effects of nitrogenous compounds (tryptone and glutamate) on glucose-derived acid production by Streptococcus and Actinomyces. Acid production was evaluated using a pH-stat method under anaerobic conditions, whereas the amounts of metabolic end-products were quantified using high performance liquid chromatography. Tryptone enhanced glucose-derived acid production by up to 2.68-fold, whereas glutamate enhanced Streptococcus species only. However, neither tryptone nor glutamate altered the end-product profiles, indicating that the nitrogenous compounds stimulate the whole metabolic pathways involving in acid production from glucose, but are not actively metabolized, nor do they alter metabolic pathways. These results suggest that nitrogenous compounds in the oral cavity promote acid production by Streptococcus and Actinomyces in vivo.

  19. Glycyrrhetinic acid and its derivatives in infectious diseases

    Directory of Open Access Journals (Sweden)

    Langer Dominik

    2016-09-01

    Full Text Available Introduction. Licorice or liquorice (Glycyrrhiza glabra, Leguminosae is a perennial plant naturally occurring or cultivated in Europe and Asia. It was appreciated by many ancient cultures, and was employed within Arabic medicine and (beginning in the Middle Ages in Europe folk medicine as a remedy for many diseases. Currently, the sweet flavoured root of this plant – Radix Glycyrrhizae (Liquirtiae, is widely taken for the treating of various upper respiratory tract diseases, as well as for gastric ulcer disease. It is also utilized as a sweetening and flavouring agent in the food, tobacco and pharmacy industries. The main active ingredient of liquorice is the triterpenoid saponin, glycyrrhizin, which is a mixture of calcium, magnesium and potassium salts of glycyrrhizic acid (GA. Glycyrrhizic acid is composed of an aglycone, that is 18β-glycyrrhetinic acid (GE, and a D-glucuronic acid dimer. The aim of this review is to discuss some aspects of the activity of glycyrrhetinic acid and its derivatives in infectious diseases.

  20. Microbial Substrate Usage Indicated by C-14 Contents of Phospholipid Fatty Acids From Soil Organic Matter

    Science.gov (United States)

    Rethemeyer, J.; Nadeau, M. J.; Grootes, P. M.; Kramer, C.; Gleixner, G.

    2004-05-01

    Phospholipid fatty acids (PLFA's) are generally associated with viable (bacterial) cell membranes. They are thought to be short-lived under normal soil conditions. We compare the C-14 levels in PLFA's obtained from soil samples from the,clean" experimental site at Rotthalmünster (Germany) with those from the agricultural research station at Halle (Germany), where the soil is contaminated with,old" carbon from lignite mining and industry. The most abundant PLFA's were isolated via preparative capillary gas chromatography of their methyl-esters at the Max-Planck Institute, Jena, and their C-14 concentration was determined via accelerator mass spectrometry at the Leibniz-Labor, Kiel. The C-14 levels of three mono-unsaturated fatty acids (n-C17:1, n-C18:1 (and n-C16:1)) are not statistically significant different from those of the contemporaneous atmosphere, indicating these fatty acids were derived from fresh plant material. C-14 levels significantly above those of the atmosphere in three saturated fatty acids (i/a-C15:0, n-C16:0 and cy-C18:0) from the surface soil of Rotthalmünster must derive from carbon fixed from the atmosphere several years earlier, when levels of bomb-C-14, remaining from the atmospheric nuclear weapons tests, especially of the early 1960's, were still higher. Lower C-14 levels in the same compounds from the Halle surface soil indicate the incorporation of "old" contaminant carbon. A below- atmospheric C-14 concentration in n-C18:0 in Rotthalmünster surface soil may reflect the partial incorporation of carbon from older, pre-bomb times. The C-14 concentrations show these PLFA's were synthesized predominantly from recent to sub-recent photosynthetic compounds, while the significant differences in C-14 concentration, observed between the PLFA's, indicate their production from soil organic matter fractions of different (recent) age and C-14 content. The Halle results show "old" carbon may be incorporated into PLFA's and thus reenter the soil

  1. Variability of basin scale water resources indicators derived from global hydrological and land surface models

    Science.gov (United States)

    Werner, Micha; Blyth, Eleanor; Schellekens, Jaap

    2016-04-01

    Global hydrological and land-surface models are becoming increasingly available, and as the resolution of these improves, as well how hydrological processes are represented, so does their potential. These offer consistent datasets at the global scale, which can be used to establish water balances and derive policy relevant indicators in medium to large basins, including those that are poorly gauged. However, differences in model structure, model parameterisation, and model forcing may result in quite different indicator values being derived, depending on the model used. In this paper we explore indicators developed using four land surface models (LSM) and five global hydrological models (GHM). Results from these models have been made available through the Earth2Observe project, a recent research initiative funded by the European Union 7th Research Framework. All models have a resolution of 0.5 arc degrees, and are forced using the same WATCH-ERA-Interim (WFDEI) meteorological re-analysis data at a daily time step for the 32 year period from 1979 to 2012. We explore three water resources indicators; an aridity index, a simplified water exploitation index; and an indicator that calculates the frequency of occurrence of root zone stress. We compare indicators derived over selected areas/basins in Europe, Colombia, Southern Africa, the Indian Subcontinent and Australia/New Zealand. The hydrological fluxes calculated show quite significant differences between the nine models, despite the common forcing dataset, with these differences reflected in the indicators subsequently derived. The results show that the variability between models is related to the different climates types, with that variability quite logically depending largely on the availability of water. Patterns are also found in the type of models that dominate different parts of the distribution of the indicator values, with LSM models providing lower values, and GHM models providing higher values in some

  2. Hydroxycinnamic acid derivatives in an aquatic liverwort as possible bioindicators of enhanced UV radiation

    Energy Technology Data Exchange (ETDEWEB)

    Arroniz-Crespo, M.; Nunez-Olivera, E. [Universidad de La Rioja, Complejo Cientifico-Tecnologico, Avda. Madre de Dios 51, 26006 Logrono (La Rioja) (Spain); Martinez-Abaigar, J. [Universidad de La Rioja, Complejo Cientifico-Tecnologico, Avda. Madre de Dios 51, 26006 Logrono (La Rioja) (Spain)], E-mail: javier.martinez@unirioja.es

    2008-01-15

    We examined, under laboratory conditions, the physiological responses of the aquatic liverwort Jungermannia exsertifolia subsp. cordifolia to artificially enhanced ultraviolet (UV) radiation for 82 days, especially considering the responses of five hydroxycinnamic acid derivatives. This species lives in mountain streams, where it is exposed to low temperatures and high UV levels, and this combination is believed to increase the adverse effects of UV. Enhanced UV radiation hardly caused any change in several physiological variables indicative of vitality, such as F{sub v}/F{sub m} and chlorophylls/phaeopigments ratio (OD430/OD410). Thus, this liverwort seemed to be tolerant to UV radiation, probably due to the accumulation of three UV-absorbing hydroxycinnamic acid derivatives: p-coumaroylmalic acid, 5''-(7'',8''-dihydroxycoumaroyl)-2-caffeoylmalic acid, and 5''-(7'',8''-dihydroxy-7-O-{beta}-glucosyl-coumaroyl)-2-caffeoylmalic acid. These compounds might serve as bioindicators of enhanced UV radiation. - Several hydroxycinnamic acid derivatives of an aquatic liverwort are induced by enhanced UV radiation and might serve as bioindicators of changes in UV levels.

  3. Antiherbivore prenylated benzoic acid derivatives from Piper kelleyi.

    Science.gov (United States)

    Jeffrey, Christopher S; Leonard, Michael D; Glassmire, Andrea E; Dodson, Craig D; Richards, Lora A; Kato, Massuo J; Dyer, Lee A

    2014-01-24

    The known prenylated benzoic acid derivative 3-geranyl-4-hydroxy-5-(3″,3″-dimethylallyl)benzoic acid (1) and two new chromane natural products were isolated from the methanolic extract of the leaves of Piper kelleyi Tepe (Piperaceae), a midcanopy tropical shrub that grows in lower montane rain forests in Ecuador and Peru. Structure determination using 1D and 2D NMR analysis led to the structure of the chromene 2 and to the reassignment of the structure of cumanensic acid as 4, an isomeric chromene previously isolated from Piper gaudichaudianum. The structure and relative configuration of new chromane 3 was determined using 1D and 2D NMR spectroscopic analysis and was found to be racemic by ECD spectropolarimetry. The biological activity of 1-3 was evaluated against a lab colony of the generalist caterpillar Spodoptera exigua (Noctuidae), and low concentrations of 2 and 3 were found to significantly reduce fitness. Further consideration of the biosynthetic relationship of the three compounds led to the proposal that 1 is converted to 2 via an oxidative process, whereas 3 is produced through hetero-[4+2] dimerization of a quinone methide derived from the chromene 2.

  4. Copper(I) mediated cross-coupling of amino acid derived organozinc reagents with acid chlorides

    DEFF Research Database (Denmark)

    Hjelmgaard, Thomas; Tanner, David Ackland

    2006-01-01

    This paper describes the development of a straightforward experimental protocol for copper-mediated cross-coupling of amino acid derived beta-amido-alkylzinc iodides 1 and 3 with a range of acid chlorides. The present method uses CuCN center dot 2LiCl as the copper source and for organozinc reagent...... 1 the methodology appears to be limited to reaction with more stable acid chlorides, providing the desired products in moderate yields. When applied to organozinc reagent 3, however, the protocol is more general and provides the products in good yields in all but one of the cases tested....

  5. Influence of organic acids on UV-Vis spectra of pyrrolidino- [60]fullerene derivatives

    Institute of Scientific and Technical Information of China (English)

    2001-01-01

    A pyrrolidino[60]fullerene 1 with pyrrolidine group was synthesized and characterized. The UV-Vis spectra showed that the blue shift of absorption peaks was first observed when strong organic acids such as p-toluene sulfonic or trifluoroacetic acid were added to the solution of pyrrolidino[60]fullerene 1 in dichloromethane. The results indicated that the pyrrolidino[60]fullerene derivatives without pyrrolidine group also possess the same phenomenon. Experiments and computation with the MOPAC 7.0 semi-em- pirical PM3 method demonstrated the reason that some energy gaps on [60]fullerene skeleton were increased because electronic charges on [60]fullerene framework transferred to pyrrolidine ring when strong organic acids were added into pyrrolidino[60]fullerene derivatives' solution; as the result, the complexes could be formed and some absorption wave-lengths blue shifted in the UV-Vis spectrum.

  6. Local solvent acidities in β-cyclodextrin complexes with PRODAN derivatives.

    Science.gov (United States)

    Naughton, Hannah R; Abelt, Christopher J

    2013-03-28

    The local solvent acidities (SA scale) of six 6-carbonyl-2-aminonaphthalene derivatives as β-cyclodextrin complexes in water are determined through fluorescence quenching. The local polarities (E(T)(N) scale) are determined through the shift of the emission center-of-mass. The apparent SA values reflect the solvent structure surrounding the guest’s carbonyl group, whereas the apparent E(T)(N) values reveal the net polarity of the entire guest molecule. Comparison of these values affords greater insight into the structures of the host–guest complexes. Derivatives 1 and 5 show unusually large acidities, indicative of highly exposed carbonyl groups. The remaining compounds give emission intensities pointing to shielded carbonyl groups. In this study, PRODAN and its derivatives are functioning as dual channel sensors of their local environment.

  7. Efficient Debromination of Vicinal (, (-Dibromo Carboxylic Acid Derivatives with the Sm/HOAc System

    Institute of Scientific and Technical Information of China (English)

    2002-01-01

    The α, β vicinal dibromo carboxylic acid and its derivatives were debrominated with Sm/HOAc system to afford the corresponding cinnamic acid and its derivatives in good yields under mild conditions.

  8. Inhibition of acidic corrosion of aluminum by triazoline derivatives

    Energy Technology Data Exchange (ETDEWEB)

    Khamis, E. (Alexandria Univ., Ibrahimia (Egypt). Dept. of Chemistry); Atea, M. (Alexandria Univ., Ibrahimia (Egypt). Dept. of Materials Science)

    1994-02-01

    Inhibition of the corrosion of aluminum (Al) in hydrochloric acid (HCl) by some triazoline derivatives was studied in relation to the concentration of the inhibitors using gasometry, the weight-loss method, and the potentiodynamic technique. All compounds investigated were found to be inhibitors of the mixed type. The inhibitory character of the additives depended upon the +R (resonance) and +I (inductive) powers of alkyl or aryl groups of the triazoline derivatives. Inhibition was ascribed to the adsorption of the inhibitor onto the metal oxide surface following the Flory-Huggins isotherm. The compounds were adsorbed on the metal surface. Each molecule of the inhibitors occupied an average of 3.8 active sites on the metal surface. The values of activation free energies varied between [minus]30 kJ/mol and [minus]45 kJ/mol.

  9. Aldehydic lipid peroxidation products derived from linoleic acid.

    Science.gov (United States)

    Spiteller, P; Kern, W; Reiner, J; Spiteller, G

    2001-04-30

    Lipid peroxidation (LPO) processes observed in diseases connected with inflammation involve mainly linoleic acid. Its primary LPO products, 9-hydroperoxy-10,12-octadecadienoic acid (9-HPODE) and 13-hydroperoxy-9,11-octadecadienoic acid (13-HPODE), decompose in multistep degradation reactions. These reactions were investigated in model studies: decomposition of either 9-HPODE or 13-HPODE by Fe(2+) catalyzed air oxidation generates (with the exception of corresponding hydroxy and oxo derivatives) identical products in often nearly equal amounts, pointing to a common intermediate. Pairs of carbonyl compounds were recognized by reacting the oxidation mixtures with pentafluorobenzylhydroxylamine. Even if a pure lipid hydroperoxide is subjected to decomposition a great variety of products is generated, since primary products suffer further transformations. Therefore pure primarily decomposition products of HPODEs were exposed to stirring in air with or without addition of iron ions. Thus we observed that primary products containing the structural element R-CH=CH-CH=CH-CH=O add water and then they are cleaved by retroaldol reactions. 2,4-Decadienal is degraded in the absence of iron ions to 2-butenal, hexanal and 5-oxodecanal. Small amounts of buten-1,4-dial were also detected. Addition of m-chloroperbenzoic acid transforms 2,4-decadienal to 4-hydroxy-2-nonenal. 4,5-Epoxy-2-decenal, synthetically available by treatment of 2,4-decadienal with dimethyldioxirane, is hydrolyzed to 4,5-dihydroxy-2-decenal.

  10. Synthesis and anticancer evaluation of alpha-lipoic acid derivatives.

    Science.gov (United States)

    Zhang, Shi-Jie; Ge, Qiu-Fu; Guo, Dian-Wu; Hu, Wei-Xiao; Liu, Hua-Zhang

    2010-05-15

    alpha-Lipoic acid derivatives were synthesized and evaluated for their in vitro anticancer activities against NCI-460, HO-8910, KB, BEL-7402, and PC-3 cell lines. The results, for most compounds exhibited dose-dependent inhibitory property and several compounds had good inhibitions at the dose of 100 microg/mL. Compound 17 m was further selected for in vivo evaluation against S180 xenograft in ICR mice, which had 24.7% tumor-weight inhibition through intragastric administration of 200mg/kg of body weight. Moreover, the LD(50) in mice for 17 m through ig exceeded 1000 mg/kg of body weight.

  11. Esterification of fermentation-derived acids via pervaporation

    Science.gov (United States)

    Datta, Rathin; Tsai, Shih-Perng

    1998-01-01

    A low temperature method for esterifying ammonium- and amine-containing salts is provided whereby the salt is reacted with an alcohol in the presence of heat and a catalyst and then subjected to a dehydration and deamination process using pervaporation. The invention also provides for a method for producing esters of fermentation derived, organic acid salt comprising first cleaving the salt into its cationic part and anionic part, mixing the anionic part with an alcohol to create a mixture; heating the mixture in the presence of a catalyst to create an ester; dehydrating the now heated mixture; and separating the ester from the now-dehydrated mixture.

  12. Banana-shaped molecules derived from substituted isophthalic acids

    Indian Academy of Sciences (India)

    H T Nguyen; J P Bedel; J C Rouillon; J P Marcerou; M F Achard

    2003-08-01

    In this paper we present a review of five-rings banana-shaped molecules derived from isophthalic acids. This study deals with about a hundred compounds and most of them have not been published. By a combination of several linking groups and different selected substituents either on the outer rings or on the central core, several mesophases with switching properties are induced. The study of homologous series underlines the importance of the length and nature of the terminal chains. X-ray analysis reveals several new structures.

  13. Azorhodanine derivatives as inhibitors for acidic corrosion of nickel.

    Science.gov (United States)

    Fouda, Abd El-Aziz S; Al-Sarawy, Ahmed A; Omar, Tark M

    2005-01-01

    Azorhodanine derivatives (HL1-HL5) were tested as corrosion inhibitors for nickel in 2M HNO3 solution using weight loss and galvanostatic polarization techniques. The results showed that these derivatives act as inhibitors for nickel in this medium. The inhibition was assumed to occur via adsorption of the inhibitor molecule on the metal surface. Polarization measurements indicated that these compounds act as mixed-type inhibitors, but the cathode is more polarized when an external current was applied. This means that these compounds retard the rate of hydrogen evolution and the rate of dissolution of the metal. Results showed that azorhodanine derivatives are adsorbed on the nickel surface following Temkin's adsorption isotherm. The activation energy and thermodynamic parameters were calculated and discussed at different temperatures (30-45 degrees C).

  14. An Alternative to Synthetic Acid Base Indicator-Tagetes Erecta Linn

    OpenAIRE

    A. Elumalai; M. C. Eswariah; M. K. Chinna; B. A. Kumar

    2012-01-01

    The present work highlights the use of the methanolic extract of the flowers of Tagetes erecta as an acid-base indicator in acid-base titrations. This natural indicator is easy to extract as well as easily available. Indicators used in titration show well marked changes of colour in certain intervals of pH. Most of these indicators are organic dyes and are of synthetic origin. Today synthetic indicators are the choice of acid-base titrations. But due to environmental pollution, availability a...

  15. Reducing ulcerogenic potential of biphenyl acetic acid: Design and development of chimeric derivatives with amino acids

    Directory of Open Access Journals (Sweden)

    Suneela Dhaneshwar

    2016-09-01

    Full Text Available In an attempt to minimize the ulcerogenic potential and associated gastro-intestinal toxicity of bioprecursor fenbufen and its active metabolite biphenyl acetic acid, carrier-linked chimeric derivatives of the latter were designed and synthesized using amino acids as the promoities. DCC coupling method was used for the synthesis of these amides. The chimeras were characterized by IR and 1H NMR. Pharmacological investigations were carried out in animal models for analgesic, anti-inflammatory, anti-arthritic and ulcerogenic activities. The chimeras exhibited high gastro-sparing effect; quick onset and longer duration of analgesia; enhanced/prolonged anti-inflammatory activity and better anti-arthritic effect than fenbufen or biphenyl acetic acid. These derivatives could be useful as a chronotherapy for rheumatoid arthritis due to their prolonged analgesic and anti-inflammatory effects.

  16. Discovery and Synthesis of Amino Acids Modified Deoxycholic Acid Derivatives and in Vitro Antiproliferative Evaluation.

    Science.gov (United States)

    Zhao, Chunhui; Zhao, Peizhe; Feng, Bin; Hou, Xiyan; Zhao, Longxuan

    2017-03-01

    A series of deoxycholic acid (DCA) derivatives bearing amino acid moiety has been synthesized and investigated for their potential antiproliferative activities. DCA derivative compounds were synthesized by a two or three step synthetic approach. Their bioactivities were evaluated using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method and Western blotting analysis on three tumor cell lines A549 (human lung cancer cell line), MCF-7 (human breast cancer cell line) and HeLa (human cervical carcinoma cell). The novel derivatives DCA3d, DCA5a, DCA5b, DCA5c, and DCA5d were found to be promising antiproliferative agents. Furthermore, DCA5b showed the greatest cytotoxic activity by induction of apoptosis. These compounds show potentiality for further optimization as antitumor drugs.

  17. 40 CFR 721.6110 - Alkyldi(alkyloxyhydroxypropyl) derivative, phosphoric acid esters, potassium salts.

    Science.gov (United States)

    2010-07-01

    ...) derivative, phosphoric acid esters, potassium salts. 721.6110 Section 721.6110 Protection of Environment...) derivative, phosphoric acid esters, potassium salts. (a) Chemical substance and significant new uses subject...) derivative, phosphoric acid esters, potassium salts (PMN P-91-818) is subject to reporting under this...

  18. Separation of Six Pyridoncarboylxic Acid Derivatives by Micellar and Microemulsion Electrokinetic Chromatography

    Institute of Scientific and Technical Information of China (English)

    2001-01-01

    Micellar and microemulsion electrokinetic chromatography (MEKC & MEEKC) separation of six closely structural pyridoncarboylxic acid derivatives were studied and compared. Both anionic surfactant sodium dodecyl sulfate (SDS) and cationic surfactant hexadecyl-trimethyl ammonium bromide (CTAB) were used to form micellar and microemulsion as pseudostation phases, respectively. The effects of the separation conditions on retention time and selectivity were studied. Good resolutions were obtained in selected systems, indicating that there is markably different selectivity between SDS and CTAB systems.

  19. Synthesis and antimicrobial activities of new higher amino acid Schiff base derivatives of 6-aminopenicillanic acid and 7-aminocephalosporanic acid

    Science.gov (United States)

    Özdemir (nee Güngör), Özlem; Gürkan, Perihan; Özçelik, Berrin; Oyardı, Özlem

    2016-02-01

    Novel β-lactam derivatives (1c-3c) (1d-3d) were produced by using 6-aminopenicillanic acid (6-APA), 7-aminocephalosporanic acid (7-ACA) and the higher amino acid Schiff bases. The synthesized compounds were characterized by elemental analysis, IR, 1H/13C NMR and UV-vis spectra. Antibacterial activities of all the higher amino acid Schiff bases (1a-3a) (1b-3b) and β-lactam derivatives were screened against three gram negative bacteria (Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853, Acinetobacter baumannii RSKK 02026), three gram positive bacteria (Staphylococcus aureus ATCC 25923, Enterococcus faecalis ATCC 07005, Bacillus subtilis ATCC 6633) and their drug-resistant isolates by using broth microdilution method. Two fungi (Candida albicans and Candida krusei) were used for antifungal activity.

  20. Infrared Spectroscopy of Hydrogen Bonds in Benzoic Acid Derivatives

    Science.gov (United States)

    Tolstorozhev, G. B.; Bel‧kov, M. V.; Skornyakov, I. V.; Bazyl, O. K.; Artyukhov, V. Ya.; Mayer, G. V.; Shadyro, O. I.; Kuzovkov, P. V.; Brinkevich, S. D.; Samovich, S. N.

    2014-03-01

    We have measured the Fourier transform IR spectra of CCl4 solutions of benzoic acid and its biologically active derivatives. We investigated the proton-acceptor properties of the studied molecules theoretically by the molecular electrostatic potential method. The calculations are compared with experimental results. Based on an estimate of the proton-acceptor properties, we give an interpretation of the specific features of the IR spectra of benzoic acid and its derivatives in the region of the O-H and C = O vibrations. The mechanisms for interactions of the molecules are determined by the nature of substituents which are added to the benzene ring in positions para and meta to the carboxyl group. We identify the conditions for appearance of intermolecular hydrogen bonds of O-H · · · O = C, O-H · · · O-H types with formation of cyclic and linear dimers. We show that intramolecular hydrogen bonds of the type O-H · · · O-CH3 prevent the hydroxyl groups from participating in intermolecular interactions.

  1. Derivatives of xanthic acid are novel antioxidants: application to synaptosomes.

    Science.gov (United States)

    Lauderback, Christopher M; Drake, Jennifer; Zhou, Daohong; Hackett, Janna M; Castegna, Alessandra; Kanski, Jaroslaw; Tsoras, Maria; Varadarajan, Sridhar; Butterfield, D Allan

    2003-04-01

    Xanthic acids have long been known to act as reducing agents. Recently, D609, a tricyclodecanol derivative of xanthic acid, has been reported to have anti-apoptotic and anti-inflammatory properties that are attributed to specific inhibition of phosphatidyl choline phospholipase C (PC-PLC). However, because oxidative stress is involved in both of these cellular responses, the possibility that xanthates may act as antioxidants was investigated in the current study. Finding that xanthates efficiently scavenge hydroxyl radicals, the mechanism by which D609 and other xanthate derivatives may protect against oxidative damage was further examined. The xanthates studied, especially D609, mimic glutathione (GSH). Xanthates scavenge hydroxyl radicals and hydrogen peroxide, form disulfide bonds (dixanthogens), and react with electrophilic products of lipid oxidation (acrolein) in a manner similar to GSH. Further, upon disulfide formation, dixanthogens are reduced by glutathione reductase to a redox active xanthate. Supporting its role as an antioxidant, D609 significantly (p < 0.01) reduces free radical-induced changes in synaptosomal lipid peroxidation (TBARs), protein oxidation (protein carbonyls), and protein conformation. Thus, in addition to inhibitory effects on PC-PLC, D609 may prevent cellular apoptotic and inflammatory cascades by acting as antioxidants and novel GSH mimics. These results are discussed with reference to potential therapeutic application of D609 in oxidative stress conditions.

  2. Derivation of Soil Line Influence on Two-Band Vegetation Indices and Vegetation Isolines

    Directory of Open Access Journals (Sweden)

    Hiroki Yoshioka

    2009-11-01

    Full Text Available This paper introduces derivations of soil line influences on two-band vegetation indices (VIs and vegetation isolines in the red and near infra-red reflectance space. Soil line variations are described as changes in the soil line parameters (slope and offset and the red reflectance of the soil surface. A general form of a VI model equation written as a ratio of two linear functions (e.g., NDVI and SAVI was assumed. It was found that relative VI variations can be approximated by a linear combination of the three soil parameters. The derived expressions imply the possibility of estimating and correcting for soil-induced bias errors in VIs and their derived biophysical parameters, caused by the assumption of a general soil line, through the use of external data sources such as regional soil maps.

  3. Application of indicators derived by remote sensing for mapping of landslide hazard and vulnerability

    Science.gov (United States)

    Eidsvig, Unni; Vidar Vangelsten, Bjørn; Geiss, Christian; Klotz, Martin; Ekseth, Kristine; Taubenböck, Hannes

    2014-05-01

    The choice and the development of methods for risk assessment of landslides depends on several factors. Important factors are the type of landslide and the elements at risk, the choice of spatial and temporal scale, the purpose of the analysis and the needs of the end-users. In addition, data availability is a major constraint, which greatly affects the type of methods and models that can be developed. Remote sensing is a promising tool for an economical and up-to-date data collection, which also could be applied to monitor the dynamic development of risk. The spatial and temporal distribution of the risk for landslides can be assessed by monitoring hazard indicators (e.g. slope height and slope angle), exposure indicators (e.g. number of houses and the total population) and vulnerability indicators (e.g. population density, settlement structures or indicators related to structural vulnerability). Several of the indicators applicable for landslide risk and vulnerability can be obtained by remote sensing techniques. However, for better results, indicators from remote sensing should be combined with other type of data. In this work, a review on the application of indicators for landslide risk assessment in explicit models as well as an assessment of end user needs was conducted in order to determine the most relevant indicators for landslide hazard and vulnerability. Lists of recommended indicators, mainly derivable from remote sensing, have been developed. These indicators are supposed to be used in risk assessment, e.g. by combining hazard, vulnerability and exposure indicators to produce risk indices. Moreover schemes for ranking, weighting and aggregation of the indicators into hazard- and vulnerability indices are provided. The research leading to these results has received funding from the European Community's Seventh Framework Programme [FP7-SPACE-2012-1] under Grant agreement No 312972 Framework to integrate Space-based and in-situ sENSing for dynamic v

  4. Infrared spectra of hydrogen-bonded salicylic acid and its derivatives : Salicylic acid and acetylsalicylic acid

    Science.gov (United States)

    Wójcik, Marek J.

    1981-11-01

    Infrared spectra of hydrogen-bonded salicylic acid, O-deutero-salicylic acid and acetylsalicylic acid crystals have been studied experimentally and theoretically. Interpretation of these spectra was based on the Witkowski-Maréchal model. Semi-quantitative agreement between experimental and theoretical spectra can be achieved with the simplest form of this model, with values of interaction parameters transferable for equivalent intermolecular hydrogen bonds.

  5. Extraction of gold, palladium, and platinum from acidic media with cyclic sulfoxide derivative

    Institute of Scientific and Technical Information of China (English)

    Songping Wu; Guobang Gu

    2007-01-01

    The extraction of gold (Ⅲ), palladium (Ⅱ), and platinum (Ⅳ) from the acidic media with the cyclic sulfoxide derivative of a-dodecyl-tetrahydrothiophene 1-oxide (dtmso) was investigated. Gold (Ⅲ), palladium (Ⅱ), and platinum (Ⅳ) could be separated from the acidic media with suitable sulfoxide concentration and acidity. The extraction reaction of gold (Ⅲ), palladium (Ⅱ) or platinum (Ⅳ) is exothermic when dtmso is used as an extracting reagent. The coordination number was studied by the slope method. The results indicate that, in high acidity, the dtmso coordination number for extracting gold (Ⅲ) or palladium (Ⅱ) is 3, and that for platinum (Ⅳ) is 2. UV and FT-IR spectra were used to analyze the structure of the complex. Gold (Ⅲ) is coordinated with the oxygen atom in S=O group in dtmso, and palladium (Ⅱ) or platinum (Ⅳ) is coordinated with the sulfur atom in S=O group in dtmso.

  6. Derivation of Relationships between Spectral Vegetation Indices from Multiple Sensors Based on Vegetation Isolines

    Directory of Open Access Journals (Sweden)

    Kenta Obata

    2012-02-01

    Full Text Available An analytical form of relationship between spectral vegetation indices (VI is derived in the context of cross calibration and translation of vegetation index products from different sensors. The derivation has been carried out based on vegetation isoline equations that relate two reflectance values observed at different wavelength ranges often represented by spectral band passes. The derivation was first introduced and explained conceptually by assuming a general functional form for VI model equation. This process is universal by which two VIs of different sensors and/or different model equations can be related conceptually. The general process was then applied to the actual case of normalized difference vegetation index (NDVI from two sensors in a framework of inter-sensor continuity. The derivation results indicate that the NDVI from one sensor can be approximated by a rational function of NDVI from the other sensor as a parameter. Similar result was obtained for the case of soil adjusted VI, enhanced VI, and two-band variance of enhanced VI.

  7. Synthesis and cholinesterase inhibition of cativic acid derivatives.

    Science.gov (United States)

    Alza, Natalia P; Richmond, Victoria; Baier, Carlos J; Freire, Eleonora; Baggio, Ricardo; Murray, Ana Paula

    2014-08-01

    Alzheimer's disease (AD) is a neurodegenerative disorder associated with memory impairment and cognitive deficit. Most of the drugs currently available for the treatment of AD are acetylcholinesterase (AChE) inhibitors. In a preliminary study, significant AChE inhibition was observed for the ethanolic extract of Grindelia ventanensis (IC₅₀=0.79 mg/mL). This result prompted us to isolate the active constituent, a normal labdane diterpenoid identified as 17-hydroxycativic acid (1), through a bioassay guided fractionation. Taking into account that 1 showed moderate inhibition of AChE (IC₅₀=21.1 μM), selectivity over butyrylcholinesterase (BChE) (IC₅₀=171.1 μM) and that it was easily obtained from the plant extract in a very good yield (0.15% w/w), we decided to prepare semisynthetic derivatives of this natural diterpenoid through simple structural modifications. A set of twenty new cativic acid derivatives (3-6) was prepared from 1 through transformations on the carboxylic group at C-15, introducing a C2-C6 linker and a tertiary amine group. They were tested for their inhibitory activity against AChE and BChE and some structure-activity relationships were outlined. The most active derivative was compound 3c, with an IC₅₀ value of 3.2 μM for AChE. Enzyme kinetic studies and docking modeling revealed that this inhibitor targeted both the catalytic active site and the peripheral anionic site of this enzyme. Furthermore, 3c showed significant inhibition of AChE activity in SH-SY5Y human neuroblastoma cells, and was non-cytotoxic.

  8. Solubility of sparingly soluble drug derivatives of anthranilic acid.

    Science.gov (United States)

    Domańska, Urszula; Pobudkowska, Aneta; Pelczarska, Aleksandra

    2011-03-24

    This work is a continuation of our systematic study of the solubility of pharmaceuticals (Pharms). All substances here are derivatives of anthranilic acid, and have an anti-inflammatory direction of action (niflumic acid, flufenamic acid, and diclofenac sodium). The basic thermal properties of pure Pharms, i.e., melting and glass-transition temperatures as well as the enthalpy of melting, have been measured with the differential scanning microcalorimetry technique (DSC). Molar volumes have been calculated with the Barton group contribution method. The equilibrium mole fraction solubilities of three pharmaceuticals were measured in a range of temperatures from 285 to 355 K in three important solvents for Pharm investigations: water, ethanol, and 1-octanol using a dynamic method and spectroscopic UV-vis method. The experimental solubility data have been correlated by means of the commonly known G(E) equation: the NRTL, with the assumption that the systems studied here have revealed simple eutectic mixtures. pK(a) precise measurement values have been investigated with the Bates-Schwarzenbach spectrophotometric method.

  9. Enhanced lignin monomer production caused by cinnamic Acid and its hydroxylated derivatives inhibits soybean root growth.

    Directory of Open Access Journals (Sweden)

    Rogério Barbosa Lima

    Full Text Available Cinnamic acid and its hydroxylated derivatives (p-coumaric, caffeic, ferulic and sinapic acids are known allelochemicals that affect the seed germination and root growth of many plant species. Recent studies have indicated that the reduction of root growth by these allelochemicals is associated with premature cell wall lignification. We hypothesized that an influx of these compounds into the phenylpropanoid pathway increases the lignin monomer content and reduces the root growth. To confirm this hypothesis, we evaluated the effects of cinnamic, p-coumaric, caffeic, ferulic and sinapic acids on soybean root growth, lignin and the composition of p-hydroxyphenyl (H, guaiacyl (G and syringyl (S monomers. To this end, three-day-old seedlings were cultivated in nutrient solution with or without allelochemical (or selective enzymatic inhibitors of the phenylpropanoid pathway in a growth chamber for 24 h. In general, the results showed that 1 cinnamic, p-coumaric, caffeic and ferulic acids reduced root growth and increased lignin content; 2 cinnamic and p-coumaric acids increased p-hydroxyphenyl (H monomer content, whereas p-coumaric, caffeic and ferulic acids increased guaiacyl (G content, and sinapic acid increased sinapyl (S content; 3 when applied in conjunction with piperonylic acid (PIP, an inhibitor of the cinnamate 4-hydroxylase, C4H, cinnamic acid reduced H, G and S contents; and 4 when applied in conjunction with 3,4-(methylenedioxycinnamic acid (MDCA, an inhibitor of the 4-coumarate:CoA ligase, 4CL, p-coumaric acid reduced H, G and S contents, whereas caffeic, ferulic and sinapic acids reduced G and S contents. These results confirm our hypothesis that exogenously applied allelochemicals are channeled into the phenylpropanoid pathway causing excessive production of lignin and its main monomers. By consequence, an enhanced stiffening of the cell wall restricts soybean root growth.

  10. Syntheses,characteristics and fluorescence properties of complexes of terbium with benzoic acid and its derivatives

    Institute of Scientific and Technical Information of China (English)

    ZHOU Zhong-cheng; SHU Wan-gen; RUAN Jian-ming; HUANG Bai-yun; LIU You-nian

    2005-01-01

    The binary complexes of terbium with benzoic acid and its derivatives (phthalic acid,iso-phthalic acid,oaminobenzoic acid,salicylic acid,sulfosalicylic acid) were synthesized and their compositions were identified by elemental analyses.UV,IR of the complexes were investigated.The UV spectra indicate that the complexes'ultraviolet absorption is mainly the ligands' absorption,but the location of peak drifts.The IR spectra show that the IR spectra of complexes are different from those of free ligands,and the band at 400-500 cm-1,due to the stretching vibration of Tb-O,is absent for free ligands.The fluorescence properties were investigated by using luminescence spectroscope,the results show that all the six complexes of terbium exhibit excellent luminescence,due to the transition from the lowest excited state 5D4 to 7F ground state manifold,the complexes of terbium with sulfosalicylic acid have the strongest fluorescence intensity,and is stronger than o-aminobenzoic acid-terbium,whose fluorescence intensity is regarded as the strongest one in the literature,and even stronger than some phosphor of terbium.

  11. Frustrated smectic liquid crystalline phases in lactic acid derivatives

    Science.gov (United States)

    Glogarová, M.; Novotná, V.

    2016-08-01

    We have prepared and studied a series of compounds with different types of molecular core and lactate unit in the chiral terminal chain. We draw a survey and comparison of their mesomorphic properties with respect to the occurrence of twist grain boundary (TGB) phases. The materials exhibit extremely wide TGBA phase more than 60K broad, unique TGBA-TGBC-SmC*-SmCA* phase sequence and unique re-entrant TGBA phase below the SmA phase. TGB phases have been induced in binary mixtures of molecules with different molecular shape and chirality (chiral lactic acid derivative and non-chiral hockey-stick mesogen). Unique effect is observed for compounds with TGBA phase, where the applied electric field transforms the planar texture into the homeotropic one, homogeneously dark in crossed polarizers. The process is analogy of the Frederiks transition so far known only for nematics. This effect, changing the bright state to the dark one, is promising for applications.

  12. Effect of vanillin and its acid and alcohol derivatives on the diphenolase activity of mushroom tyrosinase

    Directory of Open Access Journals (Sweden)

    Masoomeh Bagheri-Kalmarzi

    2012-01-01

    Full Text Available For the first time in the present study the effects of vanillin, vanillyl alcohol, vanillic acid, as well as the newly synthesized vanillin derivative, bis-vanillin, were investigated on the oxidation of dopamine hydrochloride by mushroom tyrosinase. Among them, vanillin and bis-vanillin act as activators, while vanillyl alcohol and vanillic acid exhibited inhibitory effects, the IC50 values being estimated 1.5 and 1.0 mM, respectively. These compounds were mixed inhibitors. The presence of aldehyde and metoxy groups at the meta position of aromatic compounds seems to cause them to react as tyrosinase activators, as observed in the case of vanillin and bis-vanillin. The presence of both groups in bis-vanillin results in a stronger activation effect compared to vanillin. The results indicate that the electron-withdrawing capacity of the functional group at the C-1 position is essential for the inhibitory potency of vanillin derivatives. In comparison with other benzoic acid derivatives, the results obtained in this study suggest that the relative positioning of hydroxy and methoxy groups at meta and para positions plays an important role in the inhibition effects of benzoic acids and their inhibition potency.

  13. Study of Thiosemicarbazone Derivative of Essential Fatty Acid

    OpenAIRE

    2014-01-01

    Essential fatty acids results in numerous health benefits. Only two fatty acids are known to be essential for human alpha-linolenic acid (an omega-3 fatty acid) and linoleic acid (an omega-6 fatty acid).The importance of omega-3 fatty acids for physical well-being has been recognised for several decades . Omega-3 fatty acids have anti-inflammatory, antithrombotic, antiarrhythmic and hypolipidaemic effects. Cannabis sativa (Hemp) is an angiosperm belonging to the cannabaceae family and cannabi...

  14. GOES-derived fog and low cloud indices for coastal north and central California ecological analyses

    Science.gov (United States)

    Torregrosa, Alicia; Combs, Cindy; Peters, Jeff

    2016-02-01

    Fog and low cloud cover (FLCC) strongly influences the water, energy, and nutrient flux of coastal ecosystems. Easy-to-use FLCC data are needed to quantify the impacts of FLCC on ecosystem dynamics especially during hot and dry Mediterranean climate summers. Monthly, annual, and decadal FLCC digital maps (indices) were derived for June-September 1999-2009 for coastal California, latitude 34.50°N (south of Monterey Bay) to latitude 41.95°N (north of Crescent City) from 26,000 hourly night and day Geostationary Operational Environmental Satellite (GOES) images. Monthly average FLCC ranges from winds and is lowest in the lee of major capes. FLCC advects farthest inland through low-lying NW ocean-facing valleys. At night, average total hours of FLCC are higher more frequently on land than over the ocean. The interannual FLCC coefficient of variation shows long-term geographic stability that is strongly associated with landform position. FLCC hours per day mapped contours, derived from decadal average FLCC, delineate the commonly used term "fog belt" into FLCC zones with increased locational precision. FLCC indices are available for download from the California Landscape Conservation Cooperative Climate Commons website (http://climate.calcommons.org/datasets/summertime-fog). FLCC indices can improve analyses of biogeographic and bioclimatic species distribution models; understanding meteorological mechanisms driving FLCC patterns; solar energy feasibility studies; investigations of ecohydrology, evapotranspiration, and agricultural irrigation demand; and viticulture ripening models.

  15. New Procedure to Derive the Performance Indices Associated with Reservoir Operation Rule

    Institute of Scientific and Technical Information of China (English)

    WANG Jin-wen; ZHANG Yong-chuan; ZHANG You-quan

    2002-01-01

    Stochastic dynamic programming (SDP) is extensively used in the optimization for long-term reservoir operations. Generally, both of the steady state optimal policy and its associated performance indices (PIs) for multipurpose reservoir are of prime importance. To derive the PIs there are two typical ways: simulation and probability formula. Among the disadvantages, one is that these approaches require the pre-specified operation policy. IHuminated by the convergence of objective function in SDP, a new approach, which has the advantage that its use can be concomitant with the solving of SDP, is proposed to determine the desired PIs. In the case study, its efficiency is also practically tested.

  16. CR@BaSO4: an acid rain-indicating material.

    Science.gov (United States)

    Gao, Hong-Wen; Xu, Xin-Hui

    2011-12-28

    The CR@BaSO(4) hybrid was synthesized, characterized and used as an acid rain-indicating (ARI) material. A painted ARI umbrella was discolored after exposure to simulated acid rain of pH 5 or less and returned to the initial color after the rain stopped. Such a functionalized material may make acid rain visual to remind people in real-time.

  17. 76 FR 81363 - Temperature-Indicating Devices; Thermally Processed Low-Acid Foods Packaged in Hermetically...

    Science.gov (United States)

    2011-12-28

    ... HUMAN SERVICES Food and Drug Administration 21 CFR Part 113 (formerly 2007N-0026) Temperature-Indicating Devices; Thermally Processed Low-Acid Foods Packaged in Hermetically Sealed Containers; Correction AGENCY... (76 FR 11892). The final rule amended FDA's regulations for thermally processed low-acid...

  18. Synthesis of -acylurea derivatives from carboxylic acids and ,' -dialkyl carbodiimides in water

    Indian Academy of Sciences (India)

    Ali Ramazani; Fatemeh Zeinali Nasrabadi; Aram Rezaei; Morteza Rouhani; Hamideh Ahankar; Pegah Azimzadeh Asiabi; Sang Woo Joo; Katarzyna Ślepokura; Tadeusz Lis

    2015-12-01

    Reactions of benzoic acid derivatives and ()-cinnamic acid derivatives with , '-dialkyl carbodiimide proceed smoothly at room temperature and in neutral conditions to afford -acylurea derivatives in high yields. The reaction proceeds smoothly and cleanly under mild conditions and no side reactions were observed.

  19. 40 CFR 721.10045 - Diazotized substituted heteromonocycle coupled with naphthalene sulfonic acid derivative, nickel...

    Science.gov (United States)

    2010-07-01

    ... coupled with naphthalene sulfonic acid derivative, nickel complex, alkaline salt (generic). 721.10045... derivative, nickel complex, alkaline salt (generic). (a) Chemical substance and significant new uses subject... heteromonocycle coupled with naphthalene sulfonic acid derivative, nickel complex, alkaline salt (PMN P-02-737)...

  20. Effects of Simulated Acid Rain on Main Nutritional Indicators of Three Leafy Vegetables

    Institute of Scientific and Technical Information of China (English)

    MENG He; DONG De-ming; WANG Ju; YANG Kai-ning; TIAN Lei; SUN Wei; FANG Chun-sheng

    2011-01-01

    The purpose of this paper was to identify content changes in the main nutritional indicators of three common leafy vegetables, and to provide a theoretical basis for the protection of leafy vegetables from acid rain. The experiment investigated the effects of simulated acid rain on four main nutritional indicators, including soluble sugar,total free amino acid, soluble protein and vitamin C during the application of simulated acid rain(SAR) in pakchoi( Brassica rapa chihensis), rape(Brassica campestris L.) and lettuce( Lactuca sativa Linn. var. ramnosa Hort). The vegetables were respectively exposed to SAR of pH=7.0, 5.6, 5.0, 4.0, 3.0 and a control level of pH=6.5. The concentrations of the four main nutritional indicators were determined at harvest. The results show that nutritional quality of the three leafy vegetable species decreased with the declining of pH values of SAR. The higher the acidity of SAR was, the more significant the inhibitions were. Nutritional quality of lettuce was the most affected by simulated acid rain, followed by pakchoi and rape. The change range of soluble protein content was higher than those of the other three indicators' contents, which indicates that soluble protein is most sensitive to simulated acid rain.

  1. Gallic acid and gallic acid derivatives: effects on drug metabolizing enzymes.

    Science.gov (United States)

    Ow, Yin-Yin; Stupans, Ieva

    2003-06-01

    Gallic acid and its structurally related compounds are found widely distributed in fruits and plants. Gallic acid, and its catechin derivatives are also present as one of the main phenolic components of both black and green tea. Esters of gallic acid have a diverse range of industrial uses, as antioxidants in food, in cosmetics and in the pharmaceutical industry. In addition, gallic acid is employed as a source material for inks, paints and colour developers. Studies utilising these compounds have found them to possess many potential therapeutic properties including anti-cancer and antimicrobial properties. In this review, studies of the effects of gallic acid, its esters, and gallic acid catechin derivatives on Phase I and Phase II enzymes are examined. Many published reports of the effects of the in vitro effects of gallic acid and its derivatives on drug metabolising enzymes concern effects directly on substrate (generally drug or mutagen) metabolism or indirectly through observed effects in Ames tests. In the case of the Ames test an antimutagenic effect may be observed through inhibition of CYP activation of indirectly acting mutagens and/or by scavenging of metabolically generated mutagenic electrophiles. There has been considerable interest in the in vivo effects of the gallate esters because of their incorporation into foodstuffs as antioxidants and in the catechin gallates with their potential role as chemoprotective agents. Principally an induction of Phase II enzymes has been observed however more recent studies using HepG2 cells and primary cultures of human hepatocytes provide evidence for the overall complexity of actions of individual components versus complex mixtures, such as those in food. Further systematic studies of mechanisms of induction and inhibition of drug metabolising enzymes by this group of compounds are warranted in the light of their distribution and consequent ingestion, current uses and suggested therapeutic potential. However, it

  2. Photometric indicators of visual night sky quality derived from all-sky brightness maps

    Science.gov (United States)

    Duriscoe, Dan M.

    2016-09-01

    Wide angle or fisheye cameras provide a high resolution record of artificial sky glow, which results from the scattering of escaped anthropogenic light by the atmosphere, over the sky vault in the moonless nocturnal environment. Analysis of this record yields important indicators of the extent and severity of light pollution. The following indicators were derived through numerical analysis of all-sky brightness maps: zenithal, average all-sky, median, brightest, and darkest sky brightness. In addition, horizontal and vertical illuminance, resulting from sky brightness were computed. A natural reference condition to which the anthropogenic component may be compared is proposed for each indicator, based upon an iterative analysis of a high resolution natural sky model. All-sky brightness data, calibrated in the V band by photometry of standard stars and converted to luminance, from 406 separate data sets were included in an exploratory analysis. Of these, six locations representing a wide range of severity of impact from artificial sky brightness were selected as examples and examined in detail. All-sky average brightness is the most unbiased indicator of impact to the environment, and is more sensitive and accurate in areas of slight to moderate light pollution impact than zenith brightness. Maximum vertical illuminance provides an excellent indicator of impacts to wilderness character, as does measures of the brightest portions of the sky. Zenith brightness, the workhorse of field campaigns, is compared to the other indicators and found to correlate well with horizontal illuminance, especially at relatively bright sites. The median sky brightness describes a brightness threshold for the upper half of the sky, of importance to telescopic optical astronomy. Numeric indicators, in concert with all-sky brightness maps, provide a complete assessment of visual sky quality at a site.

  3. Synthesis, Anti-Tumor and Anti-Angiogenic Activity Evaluations of Asiatic Acid Amino Acid Derivatives

    Directory of Open Access Journals (Sweden)

    Yue Jing

    2015-04-01

    Full Text Available Fifteen semi-synthetic derivatives of asiatic acid (AA have been synthesized and evaluated for their biological activities. The successful modification of these compounds at the C-2, C-3, C-23 and C-28 positions was confirmed using NMR, MS and IR spectra. Further, their anti-tumor effects were evaluated in vitro using different cancer cell lines (HeLa, HepG2, B16F10, SGC7901, A549, MCF7 and PC3, while their anti-angiogenic activities were evaluated in vivo using a larval zebrafish model. Among the derivatives, compounds 4–10 showed more potent cytotoxic and anti-angiogenic effects than AA, while compounds 11–17 had significantly less effects. The new derivative 10 was also included in finished formulations to evaluate its stability using HPLC due to its potential topical use. The derivative 10 had markedly better anti-tumor activities than both AA and other derivatives, with similar stability as its parent compound AA.

  4. Derived Trail Making Test indices: demographics and cognitive background variables across the adult life span.

    Science.gov (United States)

    Christidi, Foteini; Kararizou, Evangelia; Triantafyllou, Nikolaos; Anagnostouli, Maria; Zalonis, Ioannis

    2015-01-01

    We examined the contribution of demographics and cognitive background variables (processing speed, visuospatial skill, working memory, and interference control) on derived Trail Making Test (TMT) scores in a large sample of Greek healthy participants. We included 775 participants and administered the TMT (TMT-A and TMT-B) and the Wechsler Intelligence Adult Scale (WAIS). Direct (TMT-A & TMT-B time-to-completion) and derived [difference TMT-(B - A) & ratio TMT-(B/A)] scores were calculated. Demographics (age, age(2), education, and gender) and WAIS Full Intelligence Quotient significantly predicted the direct TMT-A (R(2) = 0.426) and TMT-B (R(2) = 0.593) scores and to a lesser extent, the derived TMT-(B - A) (R(2) = 0.343) and TMT-(B/A) (R(2) = 0.088) scores. In a subsample of 537 healthy participants who also completed the Stroop Neuropsychological Screening Test (SNST), demographics (age and education), WAIS Digit Symbol, Block Design, Arithmetic, and SNST accounted for 44.8% and 59.7% of the variance on TMT-A and TMT-B, and 32.5% and 9.6% of the variance on TMT-(B - A) and TMT-(B/A), respectively. We found minimal influence of Block Design and Arithmetic on TMT-(B - A) and an absence of significant influence of any cognitive variable on TMT-(B/A) score. Concluding, derived TMT scores are suggested as indices to detect impairment in cognitive flexibility across the adult life span, since they minimize the effect of demographics and other cognitive background variables.

  5. Investigation of molecular interactions in the complex formation of tartaric acid derivatives with di(2-ethylhexyl) phosphoric acid

    Institute of Scientific and Technical Information of China (English)

    2008-01-01

    The molecular interactions in the complex formation of two tartaric acid derivatives with di(2-ethylhexyl) phosphoric acid are investigated. The complex formation with a 1:1 stoichiometry between tartaric acid derivatives and D2EHPA can be obtained through UV-Vis titration, NMR chemical shifts and molecular dynamic simulations. Furthermore, the differences of the two complexes on the binding constants and strength of hydrogen bonds can also be determined. Such research will ideally provide insight into ways of regulating the complex forming properties of tartaric acid derivatives for composing or syn- thesizing new chiral resolving agents.

  6. Investigation of molecular interactions in the complex formation of tartaric acid derivatives with di(2-ethylhexyl) phosphoric acid

    Institute of Scientific and Technical Information of China (English)

    TAN Bin; ZHAI Zheng; LUO GuangSheng; WANG JiaDing

    2008-01-01

    The molecular interactions in the complex formation of two tartaric acid derivatives with di(2-ethylhexyl) phosphoric acid are investigated. The complex formation with a 1:1 stoichiometry between tartaric acid derivatives and D2EHPA can be obtained through UV-Vis titration, NMR chemical shifts and molecular dynamic simulations. Furthermore, the differences of the two complexes on the binding constants and strength of hydrogen bonds can also be determined. Such research will ideally provide insight into ways of regulating the complex forming properties of tartaric acid derivatives for composing or syn-thesizing new chiral resolving agents.

  7. Chemical Reaction between Boric Acid and Phosphine Indicates Boric Acid as an Antidote for Aluminium Phosphide Poisoning

    Directory of Open Access Journals (Sweden)

    Motahareh Soltani

    2016-08-01

    Full Text Available Objectives: Aluminium phosphide (AlP is a fumigant pesticide which protects stored grains from insects and rodents. When it comes into contact with moisture, AlP releases phosphine (PH3, a highly toxic gas. No efficient antidote has been found for AlP poisoning so far and most people who are poisoned do not survive. Boric acid is a Lewis acid with an empty p orbital which accepts electrons. This study aimed to investigate the neutralisation of PH3 gas with boric acid. Methods: This study was carried out at the Baharlou Hospital, Tehran University of Medical Sciences, Tehran, Iran, between December 2013 and February 2014. The volume of released gas, rate of gas evolution and changes in pH were measured during reactions of AlP tablets with water, acidified water, saturated boric acid solution, acidified saturated boric acid solution, activated charcoal and acidified activated charcoal. Infrared spectroscopy was used to study the resulting probable adduct between PH3 and boric acid. Results: Activated charcoal significantly reduced the volume of released gas (P <0.01. Although boric acid did not significantly reduce the volume of released gas, it significantly reduced the rate of gas evolution (P <0.01. A gaseous adduct was formed in the reaction between pure AlP and boric acid. Conclusion: These findings indicate that boric acid may be an efficient and non-toxic antidote for PH3 poisoning.

  8. Chemical Reaction between Boric Acid and Phosphine Indicates Boric Acid as an Antidote for Aluminium Phosphide Poisoning

    Science.gov (United States)

    Soltani, Motahareh; Shetab-Boushehri, Seyed F.; Shetab-Boushehri, Seyed V.

    2016-01-01

    Objectives: Aluminium phosphide (AlP) is a fumigant pesticide which protects stored grains from insects and rodents. When it comes into contact with moisture, AlP releases phosphine (PH3), a highly toxic gas. No efficient antidote has been found for AlP poisoning so far and most people who are poisoned do not survive. Boric acid is a Lewis acid with an empty p orbital which accepts electrons. This study aimed to investigate the neutralisation of PH3 gas with boric acid. Methods: This study was carried out at the Baharlou Hospital, Tehran University of Medical Sciences, Tehran, Iran, between December 2013 and February 2014. The volume of released gas, rate of gas evolution and changes in pH were measured during reactions of AlP tablets with water, acidified water, saturated boric acid solution, acidified saturated boric acid solution, activated charcoal and acidified activated charcoal. Infrared spectroscopy was used to study the resulting probable adduct between PH3 and boric acid. Results: Activated charcoal significantly reduced the volume of released gas (P <0.01). Although boric acid did not significantly reduce the volume of released gas, it significantly reduced the rate of gas evolution (P <0.01). A gaseous adduct was formed in the reaction between pure AlP and boric acid. Conclusion: These findings indicate that boric acid may be an efficient and non-toxic antidote for PH3 poisoning. PMID:27606109

  9. Amino Acid Derivatives of Ligustrazine-Oleanolic Acid as New Cytotoxic Agents

    Directory of Open Access Journals (Sweden)

    Fuhao Chu

    2014-11-01

    Full Text Available A series of novel ligustrazine-oleanolic acid (TOA derivatives were designed, and synthesized by conjugating amino acids to the 3-hydroxy group of TOA by ester bonds. Their cytotoxicity was evaluated on four cancer cell lines (HepG2, HT-29, Hela and BGC-823 by standard MTT assays. The ClogP values were calculated by means of computer simulation, and logP values of both 3β-glycine ester olean-12-en-28-oic acid-3,5,6-trimethylpyrazin-2-methyl ester (6a and TOA were determined using a shake flask-ultraviolet spectrophotometry method. It was found that 6a and the 3β-L-lysine ester-6g not only displayed good cytotoxicity (IC50 < 3.5 μM but also possessed better hydrophilicity than TOA. Moreover, 6a (IC50 = 4.884 μM had lower nephrotoxicity than both 6g (IC50 = 2.310 μM and cisplatin (CDDP, IC50 = 3.691 μM on MDCK cells. Combining Giemsa and DAPI staining, it was further verified that 6a could induce HepG2 apoptosis via nuclei fragmentation and had lower nephrotoxicity. In addition, the structure-activity relationships of these derivatives are briefly discussed.

  10. Combined anticalcification treatment of bovine pericardium with decellularization and hyaluronic acid derivative.

    Science.gov (United States)

    Zhu, Deyi; Jin, Liqiang; Wang, Xuemei; Xu, Li; Liu, Tianqi

    2014-01-01

    The objective of this work was to evaluate the effect of decellularization and hyaluronic acid derivative on the improvement of anticalcification of glutaraldehyde fixed bovine pericardium (GFBP) using a rat subcutaneous implantation model A cell extraction process was employed to remove the cells and cellular components from bovine pericardium (BP), leaving a framework of largely insoluble collagen. Then acellular BP was cross-linked by glutaraldehyde solution and treated with hyaluronic acid derivative (HA-ADH) which was obtained by coupling adipic dihydrazide (ADH) on-COOH of hyaluronic acid (HA). The results of in vivo calcification tests showed that the calcium content was decreased dramatically by decellularization alone (from 28.07 ± 18.87 to 2.44 ± 0.55 μg Ca/mg dry tissue after 8 weeks' implantation), and even less concentration was shown by the combination of HA derivative treatment and decellularization (GFaBP-HA group) (0.25 ± 0.08 μg Ca/mg dry tissue after 8 weeks' implantation). In addition, GFaBP-HA group not only presented a lower degree of calcification, but also showed lower ratios of Ca/P molar, which corresponded to amorphous calcium phosphates. The obtained results indicated that GFaBP-HA was a potential candidate for the manufacture of anticalcification bioprostheses.

  11. Effects of Simulated Acid Rain on Main Nutritional Indicators of Three Leafy Vegetables

    Institute of Scientific and Technical Information of China (English)

    2011-01-01

    The purpose of this paper was to identify content changes in the main nutritional indicators of three common leafy vegetables, and to provide a theoretical basis for the protection of leafy vegetables from acid rain. The experiment investigated the effects of simulated acid rain on four main nutritional indicators, including soluble sugar, total free amino acid, soluble protein and vitamin C during the application of simulated acid rain(SAR) in pakchoi(Brassica rapa chinensis), rape(Brassica campestris L.) and lettuce(Lactuca sativa Linn. var. ramosa Hort). The vegetables were respectively exposed to SAR of pH=7.0, 5.6, 5.0, 4.0, 3.0 and a control level of pH=6.5. The concentrations of the four main nutritional indicators were determined at harvest. The results show that nutritional quality of the three leafy vegetable species decreased with the declining of pH values of SAR. The higher the acidity of SAR was, the more significant the inhibitions were. Nutritional quality of lettuce was the most affected by simulated acid rain, followed by pakchoi and rape. The change range of soluble protein content was higher than those of the other three indicators' contents, which indicates that soluble protein is most sensitive to simulated acid rain.

  12. Predicting disordered regions in proteins using the profiles of amino acid indices

    Science.gov (United States)

    Han, Pengfei; Zhang, Xiuzhen; Feng, Zhi-Ping

    2009-01-01

    Background Intrinsically unstructured or disordered proteins are common and functionally important. Prediction of disordered regions in proteins can provide useful information for understanding protein function and for high-throughput determination of protein structures. Results In this paper, algorithms are presented to predict long and short disordered regions in proteins, namely the long disordered region prediction algorithm DRaai-L and the short disordered region prediction algorithm DRaai-S. These algorithms are developed based on the Random Forest machine learning model and the profiles of amino acid indices representing various physiochemical and biochemical properties of the 20 amino acids. Conclusion Experiments on DisProt3.6 and CASP7 demonstrate that some sets of the amino acid indices have strong association with the ordered and disordered status of residues. Our algorithms based on the profiles of these amino acid indices as input features to predict disordered regions in proteins outperform that based on amino acid composition and reduced amino acid composition, and also outperform many existing algorithms. Our studies suggest that the profiles of amino acid indices combined with the Random Forest learning model is an important complementary method for pinpointing disordered regions in proteins. PMID:19208144

  13. Glutamic acid and its derivatives: candidates for rational design of anticancer drugs.

    Science.gov (United States)

    Ali, Imran; Wani, Waseem A; Haque, Ashanul; Saleem, Kishwar

    2013-05-01

    Throughout the history of human civilizations, cancer has been a major health problem. Its treatment has been interesting but challenging to scientists. Glutamic acid and its derivative glutamine are known to play interesting roles in cancer genesis, hence, it was realized that structurally variant glutamic acid derivatives may be designed and developed and, might be having antagonistic effects on cancer. The present article describes the state-of-art of glutamic acid and its derivatives as anticancer agents. Attempts have been made to explore the effectivity of drug-delivery systems based on glutamic acid for the delivery of anticancer drugs. Moreover, efforts have also been made to discuss the mechanism of action of glutamic acid derivatives as anticancer agents, clinical applications of glutamic acid derivatives, as well as recent developments and future perspectives of glutamic acid drug development have also been discussed.

  14. Buoyancy-driven instabilities of acid-base fronts: the case of a color indicator

    Science.gov (United States)

    Riolfo, L. A.; Kuster, S.; Trevelyan, P. M. J.; El Hasi, C.; Zalts, A.; Almarcha, C.; D'Onofrio, A.; de Wit, A.

    2011-11-01

    Buoyancy-driven hydrodynamic instabilities of acid-base fronts are studied both experimentally and theoretically in the case where an aqueous solution of a strong acid is put above a denser aqueous solution of a color indicator in the gravity field. The neutralization reaction between the acid and the color indicator as well as their differential diffusion modifies the initially stable density profile in the system and can trigger convective motion both above and below the initial contact line. The type of patterns observed as well as their wavelength and the speed of the reaction front are shown to depend on the value of the initial concentrations of the acid and of the color indicator and on their ratio. A reaction-diffusion model explains how the hydrodynamic instability scenarios change when the concentration of the reactants are varied.

  15. Energy densification of biomass-derived organic acids

    Science.gov (United States)

    Wheeler, M. Clayton; van Walsum, G. Peter; Schwartz, Thomas J.; van Heiningen, Adriaan

    2013-01-29

    A process for upgrading an organic acid includes neutralizing the organic acid to form a salt and thermally decomposing the resulting salt to form an energy densified product. In certain embodiments, the organic acid is levulinic acid. The process may further include upgrading the energy densified product by conversion to alcohol and subsequent dehydration.

  16. The Synthesis of Some Novel N-[a-(Isoflavone-7-O-)Acetyl ] Amino Acid Derivatives

    Institute of Scientific and Technical Information of China (English)

    2000-01-01

    A series of novel N-[(α)-(isoflavone-7-O-)acetyl] amino acid methyl esters were prepared from the efficient and regioselective alkylation of isoflavones with chloroacetyl amino acid derivatives under mild condition.

  17. Assessment of Lipophilicity Indices Derived from Retention Behavior of Antioxidant Compounds in RP-HPLC

    Directory of Open Access Journals (Sweden)

    Ioana Anamaria Sima

    2017-03-01

    Full Text Available Reverse phase high pressure liquid chromatography was employed in order to evaluate the lipophilicity of antioxidant compounds from different classes, such as phenolic acids, flavanones, flavanols, flavones, anthocyanins, stilbenes, xantonoids, and proanthocyanidins. The retention time of each compound was measured using five different HPLC columns: RP18 (LiChroCART, Purosphere RP-18e, C8 (Zorbax, Eclipse XDBC8, C16-Amide (Discovery RP-Amide C16, CN100 (Saulentechnik, Lichrosphere, and pentafluorophenyl (Phenomenex, Kinetex PFP, and the mobile phase consisted of methanol and water (0.1% formic acid in different proportions. The measurements were conducted at two different column temperatures, room temperature (22 °C and, in order to mimic the environment from the human body, 37 °C. Furthermore, principal component analysis (PCA was used to obtain new lipophilicity indices and holistic lipophilicity charts. Additionally, highly representative depictions of the chromatographic behavior of the investigated compounds and stationary phases at different temperatures were obtained using two new chemometric approaches, namely two-way joining cluster analysis and sum of ranking differences.

  18. Assessment of Lipophilicity Indices Derived from Retention Behavior of Antioxidant Compounds in RP-HPLC.

    Science.gov (United States)

    Sima, Ioana Anamaria; Kot-Wasik, Agata; Wasik, Andrzej; Namieśnik, Jacek; Sârbu, Costel

    2017-03-29

    Reverse phase high pressure liquid chromatography was employed in order to evaluate the lipophilicity of antioxidant compounds from different classes, such as phenolic acids, flavanones, flavanols, flavones, anthocyanins, stilbenes, xantonoids, and proanthocyanidins. The retention time of each compound was measured using five different HPLC columns: RP18 (LiChroCART, Purosphere RP-18e), C8 (Zorbax, Eclipse XDBC8), C16-Amide (Discovery RP-Amide C16), CN100 (Saulentechnik, Lichrosphere), and pentafluorophenyl (Phenomenex, Kinetex PFP), and the mobile phase consisted of methanol and water (0.1% formic acid) in different proportions. The measurements were conducted at two different column temperatures, room temperature (22 °C) and, in order to mimic the environment from the human body, 37 °C. Furthermore, principal component analysis (PCA) was used to obtain new lipophilicity indices and holistic lipophilicity charts. Additionally, highly representative depictions of the chromatographic behavior of the investigated compounds and stationary phases at different temperatures were obtained using two new chemometric approaches, namely two-way joining cluster analysis and sum of ranking differences.

  19. A Combined Satellite-Derived Drought Indicator to Support Humanitarian Aid Organizations

    Directory of Open Access Journals (Sweden)

    Markus Enenkel

    2016-04-01

    Full Text Available Governments, aid organizations and researchers are struggling with the complexity of detecting and monitoring drought events, which leads to weaknesses regarding the translation of early warnings into action. Embedded in an advanced decision-support framework for Doctors without Borders (Médecins sans Frontières, this study focuses on identifying the added-value of combining different satellite-derived datasets for drought monitoring and forecasting in Ethiopia. The core of the study is the improvement of an existing drought index via methodical adaptations and the integration of various satellite-derived datasets. The resulting Enhanced Combined Drought Index (ECDI links four input datasets (rainfall, soil moisture, land surface temperature and vegetation status. The respective weight of each input dataset is calculated for every grid point at a spatial resolution of 0.25 degrees (roughly 28 kilometers. In the case of data gaps in one input dataset, the weights are automatically redistributed to other available variables. Ranking the years 1992 to 2014 according to the ECDI-based warning levels allows for the identification of all large-scale drought events in Ethiopia. Our results also indicate a good match between the ECDI-based drought warning levels and reported drought impacts for both the start and the end of the season.

  20. Separation of mandelic acid and its derivatives with new immobilized cellulose chiral stationary phase

    Institute of Scientific and Technical Information of China (English)

    Jie ZHOU; Qian LIU; Guang-jun FU; Zhen-zhong ZHANG

    2013-01-01

    A new liquid chromatographic method has been developed for the chiral separation of the enantiomers of mandelic acid and their derivatives 2-chloromandelic acid,4-hydroxymandelic acid,4-methoxymandelic acid,and 3,4,5-trismethoxymandelic acid.The enantiomers were separated by a CHIRALPAK(R) IC (250 mm×4.6 mm,5 μm).Mandelic acid,4-methoxymandelic acid,and 3,4,5-trismethoxymandelic acid were baseline resolved (resolution factor (Rs)=2.21,Rs=2.14,and Rs=3.70,respectively).In contrast,the enantioselectivities between CHIRALPAK(R) IC and 2-chloromandelic acid and 4-hydroxymandelic acid investigated were low.By comparing the chromatographs of mandelic acid enantiomers and mandelic acid spiked with (R)-mandelic acid,it was determined that the first effluent was (R)-mandelic acid.

  1. Role of mitochondria in programmed cell death mediated by arachidonic acid-derived eicosanoids.

    Science.gov (United States)

    Yin, Huiyong; Zhou, Yunhua; Zhu, Mingjiang; Hou, Sarina; Li, Zi; Zhong, Huiqin; Lu, Jianhong; Meng, Tao; Wang, Junhong; Xia, Lin; Xu, Yue; Wu, Yuncheng

    2013-05-01

    Arachidonic acid-derived eicosanoids from cyclooxygenases, lipoxygenases, and cytochrome P450 are important lipid mediators involved in numerous homeostatic and pathophysiological processes. Most eicosanoids act primarily on their respective cell surface G-protein coupled receptors to elicit downstream signaling in an autocrine and paracrine fashion. Emerging evidence indicates that these hormones are also critical in apoptosis in a cell/tissue specific manner. In this review, we summarize the formation of eicosanoids and their roles as mediators in apoptosis, specifically on the roles of mitochondria in mediating these events and the signaling pathways involved. The biological relevance of eicosanoid-mediated apoptosis is also discussed.

  2. Chiral gels derived from secondary ammonium salts of (1R,3S-(+-camphoric acid

    Directory of Open Access Journals (Sweden)

    Tapas Kumar Adalder

    2010-09-01

    Full Text Available In order to have access to chiral gels, a series of salts derived from (1R,3S-(+-camphoric acid and various secondary amines were prepared based on supramolecular synthon rationale. Out of seven salts prepared, two showed moderate gelation abilities. The gels were characterized by differential scanning calorimetry, table top rheology, scanning electron microscopy, single crystal and powder X-ray diffraction. Structure property correlation based on X-ray diffraction techniques remain inconclusive indicating that some of the integrated part associated with the gelation phenomena requires a better understanding.

  3. The utility of uric acid assay in dogs as an indicator of functional hepatic mass

    Directory of Open Access Journals (Sweden)

    J. M. Hill

    2011-04-01

    Full Text Available Uric acid was used as a test for liver disease before the advent of enzymology. Three old studies criticised uric acid as a test of liver function. Uric acid, as an end-product of purine metabolism in the liver, deserved re-evaluation as a liver function test. Serumtotal bile acids are widely accepted as the most reliable liver function test. This study compared the ability of serumuric acid concentration to assess liver function with that of serumpre-prandial bile acids in dogs. In addition, due to the renal excretion of uric acid the 2 assays were also compared in a renal disease group. Using a control group of healthy dogs, a group of dogs with congenital vascular liver disease, a group of dogs with non-vascular parenchymal liver diseases and a renal disease group, the ability of uric acid and pre-prandial bile acids was compared to detect reduced functional hepatic mass overall and in the vascular or parenchymal liver disease groups separately. Sensitivities, specificities and predictive value parameters were calculated for each test. The medians of uric acid concentration did not differ significantly between any of the groups, whereas pre-prandial bile acids medians were significantly higher in the liver disease groups compared with the normal and renal disease group of dogs. The sensitivity of uric acid in detecting liver disease overall was 65% while the specificity of uric acid in detecting liver disease overall was 59 %. The sensitivity and specificity of uric acid in detecting congenital vascular liver disease was 68%and 59 %, respectively. The sensitivity and specificity of uric acid in detecting parenchymal liver disease was 63%and 60 %, respectively. The overall positive and negative predictive values for uric acid in detecting liver disease were poor and the data in this study indicated uric acid to be an unreliable test of liver function. In dogs suffering from renal compromise serum uric acid concentrations may increase into the

  4. Effects of drying on caffeoylquinic acid derivative content and antioxidant capacity of sweet potato leaves

    Directory of Open Access Journals (Sweden)

    Toong Long Jeng

    2015-12-01

    Full Text Available Caffeoylquinic acid (CQA derivatives are known to possess antioxidative potential and have many beneficial effects on human health. The present study compared the CQA contents and antioxidant activities of aerial parts of sweet potato plants. The effects of drying methods (freeze drying, and drying at 30°C, 70°C, and 100°C on these two parameters of the first fully expanded leaves were also assessed. The results indicated that the CQA derivatives were detectable in leaves, stem, and flowers of sweet potato plants (varied from 39.34 mg/g dry weight to 154.05 mg/g dry weight, with the leaves (particularly expanding and first fully expanded leaves containing more CQA derivatives than other aerial plant parts. The expanding and first fully expanded leaves also exhibited greater antioxidant activities than other aerial plant parts, possibly due to their higher contents of CQA derivatives. Drying method significantly affected the content of CQA derivatives in dried sweet potato leaf tissues. Drying treatments at both 70°C and 100°C significantly reduced the CQA derivative content and antioxidant activity in the first fully expanded leaves. Among the tested drying methods, the freeze-drying method demonstrated the preservation of the highest amount of CQA derivatives (147.84 mg/g and antioxidant property. However, 30°C cool air drying was also a desirable choice (total CQA derivative content was reduced to only 129.52 mg/g, compared to 70°C and 100°C hot air drying, for commercial-scale processing of sweet potato leaves, if the higher operation cost of freeze drying was a major concern.

  5. On the Influence of the Data Sampling Interval on Computer-Derived K-Indices

    Directory of Open Access Journals (Sweden)

    A Bernard

    2011-06-01

    Full Text Available The K index was devised by Bartels et al. (1939 to provide an objective monitoring of irregular geomagnetic activity. The K index was then routinely used to monitor the magnetic activity at permanent magnetic observatories as well as at temporary stations. The increasing number of digital and sometimes unmanned observatories and the creation of INTERMAGNET put the question of computer production of K at the centre of the debate. Four algorithms were selected during the Vienna meeting (1991 and endorsed by IAGA for the computer production of K indices. We used one of them (FMI algorithm to investigate the impact of the geomagnetic data sampling interval on computer produced K values through the comparison of the computer derived K values for the period 2009, January 1st to 2010, May 31st at the Port-aux-Francais magnetic observatory using magnetic data series with different sampling rates (the smaller: 1 second; the larger: 1 minute. The impact is investigated on both 3-hour range values and K indices data series, as a function of the activity level for low and moderate geomagnetic activity.

  6. Physico-Chemical and Structural Interpretation of Discrete Derivative Indices on N-Tuples Atoms

    Directory of Open Access Journals (Sweden)

    Oscar Martínez-Santiago

    2016-05-01

    Full Text Available This report examines the interpretation of the Graph Derivative Indices (GDIs from three different perspectives (i.e., in structural, steric and electronic terms. It is found that the individual vertex frequencies may be expressed in terms of the geometrical and electronic reactivity of the atoms and bonds, respectively. On the other hand, it is demonstrated that the GDIs are sensitive to progressive structural modifications in terms of: size, ramifications, electronic richness, conjugation effects and molecular symmetry. Moreover, it is observed that the GDIs quantify the interaction capacity among molecules and codify information on the activation entropy. A structure property relationship study reveals that there exists a direct correspondence between the individual frequencies of atoms and Hückel’s Free Valence, as well as between the atomic GDIs and the chemical shift in NMR, which collectively validates the theory that these indices codify steric and electronic information of the atoms in a molecule. Taking in consideration the regularity and coherence found in experiments performed with the GDIs, it is possible to say that GDIs possess plausible interpretation in structural and physicochemical terms.

  7. Physico-Chemical and Structural Interpretation of Discrete Derivative Indices on N-Tuples Atoms

    Science.gov (United States)

    Martínez-Santiago, Oscar; Marrero-Ponce, Yovani; Barigye, Stephen J.; Le Thi Thu, Huong; Torres, F. Javier; Zambrano, Cesar H.; Muñiz Olite, Jorge L.; Cruz-Monteagudo, Maykel; Vivas-Reyes, Ricardo; Vázquez Infante, Liliana; Artiles Martínez, Luis M.

    2016-01-01

    This report examines the interpretation of the Graph Derivative Indices (GDIs) from three different perspectives (i.e., in structural, steric and electronic terms). It is found that the individual vertex frequencies may be expressed in terms of the geometrical and electronic reactivity of the atoms and bonds, respectively. On the other hand, it is demonstrated that the GDIs are sensitive to progressive structural modifications in terms of: size, ramifications, electronic richness, conjugation effects and molecular symmetry. Moreover, it is observed that the GDIs quantify the interaction capacity among molecules and codify information on the activation entropy. A structure property relationship study reveals that there exists a direct correspondence between the individual frequencies of atoms and Hückel’s Free Valence, as well as between the atomic GDIs and the chemical shift in NMR, which collectively validates the theory that these indices codify steric and electronic information of the atoms in a molecule. Taking in consideration the regularity and coherence found in experiments performed with the GDIs, it is possible to say that GDIs possess plausible interpretation in structural and physicochemical terms. PMID:27240357

  8. Epilithic algae as indicators of biological recovery in acid-stresed lakes

    Energy Technology Data Exchange (ETDEWEB)

    Vinebrooke, R.D.

    1993-01-01

    The responsiveness of benthic algae to lake acidification and chemical recovery prompted a survey of epilithic algae along an acid-stressed lake gradient. A primary acid-stress recovery gradient, best defined by increasing dissolved inorganic carbon, was characterized by increasing epilithic algal production, and a shift from an Actinotaenium cucurbita/Fragilaria acidobiontica/Homoeothrix juliana/Zygogonium ericetorum to an Achnanthes minutissima/Cymbella spp./Gomphonema spp. indicator assemblage. Increased total, filamentous green, and desmid production, and a shift towards a placoderm desmid-dominated community, typified a secondary recovery gradient defined by increasing water colour. A reciprocal transplant experiment indicated that physiological tolerance of acid-stress was the primary ecological mechanism regulating epilithic algal production and community structure. Macrograzing was of secondary importance, affecting community architecture and species composition only in low acid-stressed habitats. Tadpoles reduced the growth of metaphyton-forming epilithic algae by selective removal of loosely attached filaments of zygnematacean genera. Metaphytic algae from two lakes of different acid-stress levels had contrasting acidity and aluminium tolerance ranges. Z. ericetorum had both a low pH optimum and relative growth rate, along with high aluminium resistance, while a less acidophilic Z. tunetanum exhibited faster growth over a broader range of acidities, but also sensitivity to aluminium concentrations in excess of naturally occurring background levels. 172 refs., 30 figs., 11 tabs.

  9. Ecosystem evaluation (1989-2012) of Ramsar wetland Deepor Beel using satellite-derived indices.

    Science.gov (United States)

    Mozumder, Chitrini; Tripathi, N K; Tipdecho, Taravudh

    2014-11-01

    The unprecedented urban growth especially in developing countries has laid immense pressure on wetlands, finally threatening their existence altogether. A long-term monitoring of wetland ecosystems is the basis of planning conservation measures for a sustainable development. Deepor Beel, a Ramsar wetland and major storm water basin of the River Brahmaputra in the northeastern region of India, needs particular attention due to its constant degradation over the past decades. A rule-based classification algorithm was developed using Landsat (2011)-derived indices, namely Normalised Difference Water Index (NDWI), Modified Normalised Difference Water Index (MNDWI), Normalised Difference Pond Index (NDPI), Normalised Difference Vegetation Index (NDVI) and field data as ancillary information. Field data, ALOS AVNIR and Google Earth images were used for accuracy assessment. A fuzzy accuracy assessment of the classified data sets showed an overall accuracy of 82 % for MAX criteria and 90 % for RIGHT criteria. The rules were used to classify major wetland cover types during low water season (January) in 1989, 2001 and 2012. The statistical analysis of the classified wetland showed heavy manifestation in aquatic vegetation and other features indicating severe eutrophication over the past 23 years. This degradation was closely related to major contributing anthropogenic factors, such as a railway line construction, growing croplands, waste disposal and illegal human settlements in the wetland catchment. In addition, the landscape development index (LDI) indicated a rapid increase in the impact of the surrounding land use on the wetland from 1989 to 2012. The techniques and results from this study may prove useful for top-down landscape analyses of this and other freshwater wetlands.

  10. Versatile Biodegradable Poly(ester amides Derived from α-Amino Acids for Vascular Tissue Engineering

    Directory of Open Access Journals (Sweden)

    Pooneh Karimi

    2010-03-01

    Full Text Available Biodegradable poly(ester amide (PEA biomaterials derived from α-amino acids, diols, and diacids are promising materials for biomedical applications such as tissue engineering and drug delivery because of their optimized properties and susceptibility for either hydrolytic or enzymatic degradation. The objective of this work was to synthesize and characterize biodegradable PEAs based on the α-amino acids L-phenylalanine and L-methionine. Four different PEAs were prepared using 1,4-butanediol, 1,6-hexanediol, and sebacic acid by interfacial polymerization. High molecular weight PEAs with narrow polydispersity indices and excellent film-forming properties were obtained. The incubation of these PEAs in PBS and chymotrypsin indicated that the polymers are biodegradable. Human coronary artery smooth muscle cells were cultured on PEA films for 48 h and the results showed a well-spread morphology. Porous 3D scaffolds fabricated from these PEAs were found to have excellent porosities indicating the utility of these polymers for vascular tissue engineering.

  11. Lanthanum(III) and praseodymium(III) derivatives with dithiocarbamates derived from α-amino acids

    Science.gov (United States)

    Rai, Anita; Sengupta, Soumitra K.; Pandey, Om P.

    2006-06-01

    Lanthanum(III) and praseodymium(III) complexes with dithiocarbamates have been synthesized by the reactions of lanthanum(III) and praseodymium(III) chloride with barium dithiocarbamate and complexes of type [LnCl(L)H 2O] n have been obtained (where Ln = La(III) or Pr(III); L = barium salt of dithiocarbamate derived from glycine, L-leucine, L-valine, DL-alanine). The complexes have been characterized by elemental analysis, molar conductance, electronic absorption and fluorescence, infrared, far infrared, 1H NMR spectral studies. The presence of coordinated water molecule is inferred from thermogravimetric analysis which indicates the loss of one water molecule at 150-170 °C. The oscillator strength, Judd-Ofelt intensity parameter, stimulated emission cross-section, etc. have been obtained for different transitions of Pr 3+.

  12. Solvatochromic behavior of the electronic absorption spectra of gallic acid and some of its azo derivatives

    Science.gov (United States)

    Masoud, Mamdouh S.; Hagagg, Sawsan S.; Ali, Alaa E.; Nasr, Nessma M.

    The electronic absorption spectra of gallic acid and its azo derivatives have been studied in various solvents of different polarities. Multiple regression techniques were applied to calculate the regression and correlation coefficients based on an equation that relates the wavenumbers of the absorption band maxima (υmax-) to the solvent parameters; refractive index (n), dielectric constant (D), empirical Kamlet-Taft solvent parameters, π*(dipolarity/polarizability), α (solvent hydrogen-bond donor acidity) and β (solvent hydrogen-bond acceptor basicity). The fitting coefficient obtained from this analysis allows estimating the contribution of each type of interactions relative to total spectral shifts in solution. The dependence of υmax- on the solvent parameters indicates that the obtained bands are affected by specific and non-specific solute-solvent interactions.

  13. Preparation and Physical Properties of Chitosan Benzoic Acid Derivatives Using a Phosphoryl Mixed Anhydride System

    Directory of Open Access Journals (Sweden)

    Kyu Yun Chai

    2012-02-01

    Full Text Available Direct benzoylation of the two hydroxyl groups on chitosan was achieved using a phosphoryl mixed anhydride system, derived from trifluoroacetic anhydride (TFAA, benzoic acids (BAs, and phosphoric acid (PA. The reaction is operated as a one pot process under mild conditions that does not require neither an inert atmosphere nor dry solvents. The structures of the synthesized compounds were confirmed by NMR and IR spectroscopy. Solubility tests on the products revealed that they were soluble in organic solvents such as N,N-dimethylformamide (DMF, dimethylsulfoxide (DMSO, and acetone. In the meantime, a morphological study by scanning electron microscopy (SEM evidently indicated that the chitosan benzoates underwent significant structural changes after the benzoylation.

  14. Resolution Enhancement of MODIS-Derived Water Indices for Studying Persistent Flooding

    Science.gov (United States)

    Underwood, L. W.; Kalcic, Maria; Fletcher, Rose

    2012-01-01

    Monitoring coastal marshes for persistent flooding and salinity stress is a high priority issue in Louisiana. Remote sensing can identify environmental variables that can be indicators of marsh habitat conditions, and offer timely and relatively accurate information for aiding wetland vegetation management. Monitoring activity accuracy is often limited by mixed pixels which occur when areas represented by the pixel encompasses more than one cover type. Mixtures of marsh grasses and open water in 250m Moderate Resolution Imaging Spectroradiometer (MODIS) data can impede flood area estimation. Flood mapping of such mixtures requires finer spatial resolution data to better represent the cover type composition within 250m MODIS pixel. Fusion of MODIS and Landsat can improve both spectral and temporal resolution of time series products to resolve rapid changes from forcing mechanisms like hurricane winds and storm surge. For this study, using a method for estimating sub-pixel values from a MODIS time series of a Normalized Difference Water Index (NDWI), using temporal weighting, was implemented to map persistent flooding in Louisiana coastal marshes. Ordinarily NDWI computed from daily 250m MODIS pixels represents a mixture of fragmented marshes and water. Here, sub-pixel NDWI values were derived for MODIS data using Landsat 30-m data. Each MODIS pixel was disaggregated into a mixture of the eight cover types according to the classified image pixels falling inside the MODIS pixel. The Landsat pixel means for each cover type inside a MODIS pixel were computed for the Landsat data preceding the MODIS image in time and for the Landsat data succeeding the MODIS image. The Landsat data were then weighted exponentially according to closeness in date to the MODIS data. The reconstructed MODIS data were produced by summing the product of fractional cover type with estimated NDWI values within each cover type. A new daily time series was produced using both the reconstructed 250

  15. Utilization of acidic α-amino acids as acyl donors: an effective stereo-controllable synthesis of aryl-keto α-amino acids and their derivatives.

    Science.gov (United States)

    Wang, Lei; Murai, Yuta; Yoshida, Takuma; Okamoto, Masashi; Tachrim, Zetryana Puteri; Hashidoko, Yasuyuki; Hashimoto, Makoto

    2014-05-16

    Aryl-keto-containing α-amino acids are of great importance in organic chemistry and biochemistry. They are valuable intermediates for the construction of hydroxyl α-amino acids, nonproteinogenic α-amino acids, as well as other biofunctional components. Friedel-Crafts acylation is an effective method to prepare aryl-keto derivatives. In this review, we summarize the preparation of aryl-keto containing α-amino acids by Friedel-Crafts acylation using acidic α-amino acids as acyl-donors and Lewis acids or Brönsted acids as catalysts.

  16. Salicylic acid and some of its derivatives as antibacterial agents for viscose fabric.

    Science.gov (United States)

    Kantouch, A; El-Sayed, A Atef; Salama, M; El-Kheir, A Abou; Mowafi, S

    2013-11-01

    Salicylic acid and three of its derivatives were used to provide antibacterial properties to viscose fabrics. The four bactericides used were bonded to the viscose fabrics using epichlorohydrin or polymer binders. Optimization of the salicylic acid and its derivatives as well as the concentration of polymers was reported. The ability of the polymer binders to attract and bind the four bactericides was observed. The overall results show that the antibacterial reactivity of salicylic acid and its derivatives are in the following order 5-bromosalicylic acid>salicylic acid>5-chlorosalicylic acid>4-chlorosalicylic acid. Using epichlorohydrin as a binding agent, unfortunately, inhibits the bactericidal activity of the four bactericides. The FTIR study concludes that the reaction between salicylic acid as well as its derivatives with epichlorohydrin takes place through the phenolic group of the acids. The unexpected deterioration in the bactericidal properties of salicylic acid and its derivatives as a result of the treatment with epichlorohydrin could be due to the nature of interaction between the epichlorohydrin molecule and the acids molecules. PVP and PU show superior ability to sustain the four bactericides used even after 10 washing cycles.

  17. CATALYTIC HYDROGENATION AND OXIDATION OF BIOMASS-DERIVED LEVULINIC ACID

    Directory of Open Access Journals (Sweden)

    Yan Gong

    2011-02-01

    Full Text Available Levulinic acid (LA, 4-oxo-pentanoic acid, is a new platform chemical with various potential uses. In this paper, catalytic hydrogenation and oxidation of levulinic acid were studied. It was shown from experiments that levulinic acid can be hydrogenated to γ-valerolactone (GVL over transition metal catalysts and oxidative-decarboxylated to 2-butanone (methyl-ethyl-ketone, MEK and methyl-vinyl-ketone (MVK by cupric oxide (CuO, cupric oxide/cerium oxide (CuO/CeO2, cupric oxide/ alumina (CuO/ Al2O3, and silver(I/ peroxydisulfate (Ag(I/S2O82-.

  18. Prompt Proxy Mapping of Flood Damaged Rice Fields Using MODIS-Derived Indices

    Directory of Open Access Journals (Sweden)

    Youngjoo Kwak

    2015-11-01

    Full Text Available Flood mapping, particularly hazard and risk mapping, is an imperative process and a fundamental part of emergency response and risk management. This paper aims to produce a flood risk proxy map of damaged rice fields over the whole of Bangladesh, where monsoon river floods are dominant and frequent, affecting over 80% of the total population. This proxy risk map was developed to meet the request of the government on a national level. This study represents a rapid, straightforward methodology for estimating rice-crop damage in flood areas of Bangladesh during the large flood from July to September 2007, despite the lack of primary data. We improved a water detection algorithm to achieve a better discrimination capacity to discern flood areas by using a modified land surface water index (MLSWI. Then, rice fields were estimated utilizing a hybrid rice field map from land-cover classification and MODIS-derived indices, such as the normalized difference vegetation index (NDVI and enhanced vegetation index (EVI. The results showed that the developed method is capable of providing instant, comprehensive, nationwide mapping of flood risks, such as rice field damage. The detected flood areas and damaged rice fields during the 2007 flood were verified by comparing them with the Advanced Land Observing Satellite (ALOS AVNIR-2 images (a 10 m spatial resolution and in situ field survey data with moderate agreement (K = 0.57.

  19. Comparative QSAR studies on toxicity of phenol derivatives using quantum topological molecular similarity indices.

    Science.gov (United States)

    Hemmateenejad, Bahram; Mehdipour, Ahmad R; Miri, Ramin; Shamsipur, Mojtaba

    2010-05-01

    Quantitative structure activity relationship (QSAR) analyses using a novel type of electronic descriptors called quantum topological molecular similarity (QTMS) indices were operated to describe and compare the mechanisms of toxicity of phenols toward five different strains (i.e., Tetrahymena pyriformis, L1210 Leukemia, Pseudomonas putida, Raja japonica and Cucumis sativus). The appropriate QSAR models for the toxicity data were obtained separately employing partial least squares (PLS) regression combined with genetic algorithms (GA), as a variable selection method. The resulting QSAR models were used to identify molecular fragments of phenol derivatives whose electronic properties contribute significantly to the observed toxicities. Using this information, it was feasible to discriminate between the mechanisms of action of phenol toxicity to the studied strains. It was found that toxicities of phenols to all strains, except with L1210 Leukemia, are significantly affected by electronic features of the phenolic hydroxyl group (C-O-H). Meanwhile, the resulting models can describe the inductive and resonance effects of substituents on various toxicities.

  20. Aqueous extracts of Mozambican plants as alternative and environmentally safe acid-base indicators.

    Science.gov (United States)

    Macuvele, Domingos Lusitaneo Pier; Sithole, Gerre Zebedias Samo; Cesca, Karina; Macuvele, Suzana Lília Pinare; Matsinhe, Jonas Valente

    2016-06-01

    Indicators are substances that change color as the pH of the medium. Many of these substances are dyes of synthetic origin. The mulala plant (Euclea natalensis), which roots are commonly used by rural communities for their oral hygiene, and roseira (Hibiscus rosa-sinensis), an ornamental plant, are abundant in Mozambique. Currently, synthetic acid-base indicators are most commonly used but have environmental implications and, on the other hand, are expensive products, so the demand for natural indicators started. This study investigated the applicability of aqueous extracts of H. rosa-sinensis and E. natalensis as acid-base indicators. Ground on this work, the extracts can be used as acid-base indicators. On the basis of the absorption spectroscopy in both the UV-Vis region and previous studies, it was possible to preliminarily pinpoint anthocyanins and naphthoquinones as responsible for the shifting of colors depending on the pH range of aqueous extracts of H. rosa-sinensis and E. natalensis. These natural indicators are easily accessible, inexpensive, easy to extract, environmentally safe, and locally available.

  1. Analysis of Citric Acid in Beverages: Use of an Indicator Displacement Assay

    Science.gov (United States)

    Umali, Alona P.; Anslyn, Eric V.; Wright, Aaron T.; Blieden, Clifford R.; Smith, Carolyne K.; Tian, Tian; Truong, Jennifer A.; Crumm, Caitlin E.; Garcia, Jorge E.; Lee, Soal; Mosier, Meredith; Nguyen, Chester P.

    2010-01-01

    The use of an indicator displacement assay permits the visualization of binding events between host and guest molecules. An undergraduate laboratory experiment is described to demonstrate the technique in the determination of citric acid content in commercially available beverages such as soda pop and fruit juices. Through the technique, students…

  2. Analysis and Identification of Acid-Base Indicator Dyes by Thin-Layer Chromatography

    Science.gov (United States)

    Clark, Daniel D.

    2007-01-01

    Thin-layer chromatography (TLC) is a very simple and effective technique that is used by chemists by different purposes, including the monitoring of the progress of a reaction. TLC can also be easily used for the analysis and identification of various acid-base indicator dyes.

  3. Using Acid Number as a Leading Indicator of Refrigeration and Air Conditioning System Performance

    Energy Technology Data Exchange (ETDEWEB)

    Dennis Cartlidge; Hans Schellhase

    2003-07-31

    number (TAN), which includes both mineral acids and organic acids, is therefore a useful indicator which can be used to monitor the condition of the system in order to perform remedial maintenance, when required, to prevent system failure. The critical TAN value is the acid level at which remedial action should be taken to prevent the onset of rapid acid formation which can result in system failure. The level of 0.05 mg KOH/g of oil was established for CFC/mineral oil systems based on analysis of 700 used lubricants from operating systems and failed units. There is no consensus within the refrigeration industry as to the critical TAN value for HFC/POE systems, however, the value will be higher than the CFC/mineral oil systems critical TAN value because of the much weaker organic acids produced from POE. A similar study of used POE lubricants should be performed to establish a critical TAN limit for POE systems. Titrimetric analysis per ASTM procedures is the most commonly used method to determine TAN values in lubricants in the refrigeration industry and other industries dealing with lubricating oils. For field measurements, acid test kits are often used since they provide rapid, semi-quantitative TAN results.

  4. Production and applications of carbohydrate-derived sugar acids as generic biobased chemicals.

    Science.gov (United States)

    Mehtiö, Tuomas; Toivari, Mervi; Wiebe, Marilyn G; Harlin, Ali; Penttilä, Merja; Koivula, Anu

    2016-10-01

    This review considers the chemical and biotechnological synthesis of acids that are obtained by direct oxidation of mono- or oligosaccharide, referred to as sugar acids. It focuses on sugar acids which can be readily derived from plant biomass sources and their current and future applications. The three main classes of sugar acids are aldonic, aldaric and uronic acids. Interest in organic acids derived from sugars has recently increased, as part of the interest to develop biorefineries which produce not only biofuels, but also chemicals to replace those currently derived from petroleum. More than half of the most desirable biologically produced platform chemicals are organic acids. Currently, the only sugar acid with high commercial production is d-gluconic acid. However, other sugar acids such as d-glucaric and meso-galactaric acids are being produced at a lower scale. The sugar acids have application as sequestering agents and binders, corrosion inhibitors, biodegradable chelators for pharmaceuticals and pH regulators. There is also considerable interest in the use of these molecules in the production of synthetic polymers, including polyamides, polyesters and hydrogels. Further development of these sugar acids will lead to higher volume production of the appropriate sugar acids and will help support the next generation of biorefineries.

  5. Distillation of natural fatty acids and their chemical derivatives

    Science.gov (United States)

    Well over 1,000 different fatty acids are known which are natural components of fats, oils (triacylglycerols), and other related compounds. These fatty acids can have different alkyl chain lengths, 0-6 carbon-carbon double bonds possessing cis- or trans-geometry, and can contain a variety of functio...

  6. Polyphosphorous acid catalyzed cyclization in the synthesis of cryptolepine derivatives

    Institute of Scientific and Technical Information of China (English)

    2007-01-01

    11-Oxo-10,11-dihydroxy-5H-indolo[3,2,b]quinoline7-carboxylic acid was obtained specifically by polyphosphorous acid catalyzed cyclization with optimal reaction conditions. Biological assays showed that it potentially inhibits the proteasomal chymotrypsin-like activity in vitro and suppresses breast cancer cell growth.

  7. A New β-Carboline Alkaloid and a New Derivate of Isoferulic Acid from Anemone altaica

    Institute of Scientific and Technical Information of China (English)

    Zhong Jie ZOU; Yue Sheng DONG; Jun Shan YANG

    2005-01-01

    A new β-carboline alkaloid, 4-(9H-β-carbolin-1-yl)-4-oxobutyric acid and a new derivate of isoferulic acid, (E)-3-(3-hydroxy-4-methoxyphenyl)acrylic acid carboxymethyl ester,were isolated from the roots of Anemone altaica. Their structures were determined on the basis of spectral data.

  8. Synthesis and Neurotrophic Activities of N-p-Tolyl/phenylsulfonyl L-Amino Acid Thiolester Derivatives

    Institute of Scientific and Technical Information of China (English)

    YANG Zhan-Nan; FAN Ming; YANG Xiao-Sheng; YU Zheng-Wen; HAO Xiao-Jiang

    2008-01-01

    Various N-p-tolyl/phenylsulfonyl L-amino acid thiolester derivatives were designed and synthesized according to combination of functional groups. The synthesized compounds were identified by spectral methods (1H NMR,13C NMR, MS and HRMS). Preliminary bioassays indicated that the compounds 4a, 4b, 4d, 5c, 5d, 5g, 6b and 6d showed remarkable activities and the compounds 4c, 5b and 6c showed moderate activities to inhibit anoxic damage of PC12 cells at 10 μg/mL, but the compounds 4d and 6d only showed moderate protective activities against PC12 cells at 5 μg/mL. Preliminary bioassays also indicated that the compounds 4c, 5a, 5c, 5d, 5e and 6b showed moderate activities to induce PC12-differentiation at 10 μg/mL.

  9. Assessment of spatially distributed values of Kc using vegetation indices derived from medium resolution satellite data

    Science.gov (United States)

    Greco, M.; Simoniello, T.; Lanfredi, M.; Russo, A. L.

    2010-09-01

    In the last years, the theme of suitable assessment of irrigation water supply has been raised relevant interest for both general principles of sustainable development and optimization of water resources techniques and management. About 99% of the water used in agriculture is lost by crops as evapotranspiration (ET). Thus, it becomes crucial to drive direct or indirect measurement in order to perform a suitable evaluation of water loss by evapotranspiration (i.e. actual evapotranspiration) as well as crop water status and its effect on the production. The main methods used to measure evapotranspiration are available only at field scale (Bowen ratio, eddy correlation system, soil water balance) confined to a small pilot area, generally due to expense and logistical constraints. This led over the last 50 years to the development of a large number of empirical methods to estimate evapotranspiration through different climatic and meteorological variables as well as combining models, based on aerodynamic theory and energy balance, taking into account both canopy properties and meteorological conditions. Among these, the Penman-Monteith equation seems to give the best results providing a robust and consistent method world wide accepted. Such conventional methods only provide accurate evapotranspiration assessment for a homogeneous region nearby the meteorological gauge station and cannot be extrapolated to other different sites; whereas remote sensing techniques allow for filling up such a gap. Some of these satellite techniques are based on the use of thermal band signals as inputs for energy balance equations. Another common approach is mainly based on the FAO method for estimating crop evapotranspiration, in which evapotranspiration data are multiplied by crop coefficients, Kc, derived from satellite multispectral vegetation indices obtained. The rationale behind such a link considers that Kc and vegetation indices are sensitive to both leaf area index and fractional

  10. Endothelial Differentiation of Human Adipose-Derived Stem Cells on Polyglycolic Acid/Polylactic Acid Mesh.

    Science.gov (United States)

    Deng, Meng; Gu, Yunpeng; Liu, Zhenjun; Qi, Yue; Ma, Gui E; Kang, Ning

    2015-01-01

    Adipose-derived stem cell (ADSC) is considered as a cell source potentially useful for angiogenesis in tissue engineering and regenerative medicine. This study investigated the growth and endothelial differentiation of human ADSCs on polyglycolic acid/polylactic acid (PGA/PLA) mesh compared to 2D plastic. Cell adhesion, viability, and distribution of hADSCs on PGA/PLA mesh were observed by CM-Dil labeling, live/dead staining, and SEM examination while endothelial differentiation was evaluated by flow cytometry, Ac-LDL/UEA-1 uptake assay, immunofluorescence stainings, and gene expression analysis of endothelial related markers. Results showed hADSCs gained a mature endothelial phenotype with a positive ratio of 21.4 ± 3.7% for CD31+/CD34- when induced in 3D mesh after 21 days, which was further verified by the expressions of a comprehensive range of endothelial related markers, whereas hADSCs in 2D induced and 2D/3D noninduced groups all failed to differentiate into endothelial cells. Moreover, compared to 2D groups, the expression for α-SMA was markedly suppressed in 3D cultured hADSCs. This study first demonstrated the endothelial differentiation of hADSCs on the PGA/PLA mesh and pointed out the synergistic effect of PGA/PLA 3D culture and growth factors on the acquisition of mature characteristic endothelial phenotype. We believed this study would be the initial step towards the generation of prevascularized tissue engineered constructs.

  11. Stability-indicating RP-LC method for quantification of fusidic acid in cream

    Directory of Open Access Journals (Sweden)

    Mariane Machado Curbete

    Full Text Available ABSTRACT Fusidic acid is an antibiotic steroid indicated for the treatment of infections caused by the genus Staphylococcus, including methicillin resistant Staphylococcus aureus strains, and other Gram-positive bacteria. In the present study, a stability-indicating reversed-phase liquid chromatography (RP-LC method was developed and validated for the determination of fusidic acid in dermatological cream as an alternative to existing methods. Analyses were performed using a C18 column and guard column at room temperature, eluting with an isocratic mobile phase of acetonitrile and water (72:28, v/v, adjusted to pH 3.5 with acetic acid, pumped at a flow rate of 1.0 mL min-1, detection at 210 nm and 20 µL of injection volume. The forced degradation study was conducted under acidic, alkaline, neutral, photolytic, and oxidative stress conditions. The method was validated according to ICH and FDA guidelines; it was linear, precise, accurate, selective, and robust over concentrations of 5-95 µg mL-1, with detection and quantification limits of 0.43 and 1.31 μg mL-1, respectively. Therefore, we conclude that this method is suitable for quantifying fusidic acid in pharmaceutical dermatological creams and determining its stability, representing a more economical and practical alternative for routine analysis in quality control.

  12. The relationship between serum brain-derived neurotrophic factor (BDNF) and cardiometabolic indices in schizophrenia.

    Science.gov (United States)

    Nurjono, Milawaty; Tay, Yi Hang; Lee, Jimmy

    2014-08-01

    Brain derived neurotrophic factor (BDNF), which has been implicated in the pathogenesis of schizophrenia, has been recently shown to be involved in the regulation of metabolism and energy homeostasis. This study seeks to examine the relationship between BDNF, metabolic indices and cardiovascular (CVD) risk in patients with schizophrenia. Medical histories, demographic information and anthropometric measurements were collected and analyzed from 61 participants with schizophrenia. Fasting glucose and lipids were measured in a central laboratory, and serum BDNF was analyzed using commercially available enzyme-linked immunosorbent assay (ELISA). The 10-year CVD risk for each participant was computed using the Framingham risk score (FRS). Linear regressions were performed to examine the relationships between serum BDNF with body mass index (BMI), blood pressure (BP), triglycerides (TG), total cholesterol, high-density lipoprotein cholesterol (HDL-C) and glucose. To examine the relationship between serum BDNF and FRS, serum BDNF was categorized into quartiles, and a multiple regression was performed. After adjusting for age, gender and current smoking status, diastolic BP (dBP) (p=0.045) and TG (p=0.015) were found to be significantly associated with serum BDNF. Participants in the highest quartile of serum BDNF had a 3.3 times increase in FRS over those in the lowest quartile. Our findings support the possible regulatory role of BDNF in metabolism and cardiovascular homeostasis among patients with schizophrenia similar to that observed among the non-mentally ill. Serum BDNF not only present itself as a candidate biomarker of schizophrenia but also might be a viable marker of metabolic co-morbidities associated with schizophrenia.

  13. Antibacterial activity of triterpene acids and semi-synthetic derivatives against oral pathogens.

    Science.gov (United States)

    Scalon Cunha, Luis C; Andrade e Silva, Márcio L; Cardoso Furtado, Niege A J; Vinhólis, Adriana H C; Gomes Martins, Carlos H; da Silva Filho, Ademar A; Cunha, Wilson R

    2007-01-01

    Triterpene acids (ursolic, oleanoic, gypsogenic, and sumaresinolic acids) isolated from Miconia species, along with a mixture of ursolic and oleanolic acids and a mixture of maslinic and 2-a-hydroxyursolic acids, as well as ursolic acid derivatives were evaluated against the following microorganisms: Streptococcus mutans, Streptococcus mitis, Streptococcus sanguinis, Streptococcus salivarius, Streptococcus sobrinus, and Enterococcus faecalis, which are potentially responsible for the formation of dental caries in humans. The microdilution method was used for the determination of the minimum inhibitory concentration (MIC) during the evaluation of the antibacterial activity. All the isolated compounds, mixtures, and semi-synthetic derivatives displayed activity against all the tested bacteria, showing that they are promising antiplaque and anticaries agents. Ursolic and oleanolic acids displayed the most intense antibacterial effect, with MIC values ranging from 30 microg/mL to 80 microg/mL. The MIC values of ursolic acid derivatives, as well as those obtained for the mixture of ursolic and oleanolic acids showed that these compounds do not have higher antibacterial activity when compared with the activity observed with either ursolic acid or oleanolic acid alone. With regard to the structure-activity relationship of triterpene acids and derivatives, it is suggested that both hydroxy and carboxy groups present in the triterpenes are important for their antibacterial activity against oral pathogens.

  14. Caffeoyl-D-Glucaric Acid Derivatives in the Genus Gnaphalium (Asteraceae: Gnaphalieae

    Directory of Open Access Journals (Sweden)

    Serhat Sezai Cicek

    2012-03-01

    Full Text Available A chemosystematic survey was carried out to specify whether leontopodic acid and leontopodic acid B, two unique caffeoyl-D-glucaric acid derivatives, recently identified in the emblematic alpine edelweiss (Leontopodium alpinum Cass. are also found in members of the genus Gnaphalium from the Alps. Gnaphalium is closely related to Leontopodium and both genera are assigned to the Gnaphaliinae subtribe (Asteraceae, Gnaphalieae. In all investigated Gnaphalium species, G. hoppeanum W.D.J.Koch, G. norvergicum Gunnerus, G. supinum L., G. sylvaticum L., and G. uliginosum L., both leontopodic acid and leontopodic acid B were detected. Moreover, a number of related compounds were detected by HPLC/MS and their assumed structures are discussed. The chemosystematic data reported here are of interest to explore new sources for the biologically active compounds leontopodic acid and leontopodic acid B and they also hint to the occurrence of novel caffeoyl-D-glucaric acid derivatives in Gnaphalium not detected in Leontopodium, yet.

  15. Recent Advancements and Biological Activities of Aryl Propionic Acid Derivatives: (A Review

    Directory of Open Access Journals (Sweden)

    Harshita Dhall

    2016-08-01

    Full Text Available The aryl propionic acid derivatives belong to an important class of NSAIDs (Non Steroidal Anti-inflammatory Drugs. Ibuprofen, chemically called 2-(4-isobutyl phenyl propionic acid, is a well known NSAID. Aryl propionic acid derivatives possesses a wide range of biological activities including anti-bacterial, anti-convulsant, anti-cancer, analgesic and anti-inflammatory activities. Apart from very potent compounds in the field of analgesics and antipyrectics as Ibuprofen, Oxaprozin, Ketoprofen, Fenoprofen; aryl propionic acid derivatives plays important role to treat other ailments also. Through this review, an attempt has been made to emphasize on recent work done and recent advancements in arena of aryl propionic acid derivatives in view of medicinal chemistry.

  16. Co2 chemosorption by functionalized amino acid derivatives

    DEFF Research Database (Denmark)

    2015-01-01

    The absorption and desorption behaviour of carbon dioxide (CO2) using a composition comprising an ionic compound comprising a cation [A+] and an anion [B-] is described, wherein the anion [B-] is a mono-amine functionalized amino acid.......The absorption and desorption behaviour of carbon dioxide (CO2) using a composition comprising an ionic compound comprising a cation [A+] and an anion [B-] is described, wherein the anion [B-] is a mono-amine functionalized amino acid....

  17. Antileishmanial activity of semisynthetic lupane triterpenoids betulin and betulinic acid derivatives: synergistic effects with miltefosine.

    Directory of Open Access Journals (Sweden)

    Maria C Sousa

    Full Text Available Leishmaniasis is a neglected tropical disease (NTDs, endemic in 88 countries, affecting more than 12 million people. The treatment consists in pentavalent antimony compounds, amphotericin B, pentamidine and miltefosine, among others. However, these current drugs are limited due to their toxicity, development of biological resistance, length of treatment and high cost. Thus, it is important to continue the search for new effective and less toxic treatments. The anti-Leishmania activity of sixteen semisynthetic lupane triterpenoids derivatives of betulin (BT01 to BT09 and betulinic acid (AB10 to AB16 were evaluated. Drug interactions between the active compounds and one current antileishmanial drug, miltefosine, were assessed using the fixed ratio isobologram method. In addition, effects on the cell cycle, apoptosis/necrosis events, morphology and DNA integrity were studied. The derivatives BT06 (3β-Hydroxy-(20R-lupan-29-oxo-28-yl-1H-imidazole-1-carboxylate and AB13 (28-(1H-imidazole-1-yl-3,28-dioxo-lup-1,20(29-dien-2-yl-1H-imidazole-1-carboxylate were found to be the most active, with IC50 values of 50.8 µM and 25.8 µM, respectively. Interactions between these two compounds and miltefosine were classified as synergistic, with the most effective association being between AB13 and miltefosine, where decreases of IC50 values to 6 µM were observed, similar to the miltefosine activity alone. AB13 induced significant morphological changes, while both derivatives produced anti-proliferative activity through cell cycle arrest at the G0/G1 phase. Neither of these derivatives induced significant apoptosis/necrosis, as indicated by phosphatidylserine externalization and DNA fragmentation assays. In addition, neither of the derivatives induced death in macrophage cell lines. Thus, they do not present any potential risk of toxicity for the host cells. This study has identified the betulin derivative BT06 and the betulinic acid derivative AB13 as promising

  18. Ecosystems resilience to drought: indicators derived from time-series of Earth Observation data

    Science.gov (United States)

    Garcia, Monica; Fernández, Nestor; Delibes, Miguel

    2013-04-01

    Increasing our understanding of how ecosystems differ in their vulnerability to extreme climatic events such as drought is critical. Resilient ecosystems are capable to cope with climatic perturbations retaining the same essential function, structure and feedbacks. However, if the effect of a perturbation is amplified, abrupt shifts can occur such as in desertification processes. Empirical indicators of robustness and resilience to drought events could be developed from time series of Earth Observation (EO) data. So far, the information content of EO time series for monitoring ecosystem resilience has been underutilized, being mostly limited to detection of greening or rainfall use efficiency (RUE) trends at interannual time-scales. Detection of thresholds, shifts, extremes, and hysteresis processes is still in its infancy using EO data. Only recently some studies are starting to utilize this avenue of research using vegetation indices with some controversy due to the substitution of time by space. In drylands, where ecosystem functioning is largely controlled by rainfall, a key variable for monitoring is evapotranspiration as it connects the energy, water and carbon cycles. It can be estimated using EO data using a surface energy balance approach. In this work we propose the use of new empirical indicators of resilience to drought derived from EO time series. They are extracted from analyses of lagged cross-correlations between rainfall and evapotranspiration anomalies at several time-steps. This allows elucidating as well if an observed extreme ecological response can be attributed to a climate extreme. Additionally, increases in autocorrelation have been proposed to detect losses of resilience or changes in recovery capacity from a perturbation. Our objective was to compare rates of recovery from drought of different ecosystems in the natural park of Doñana (Spain) composed of wetlands, pine forest, shrublands with and without access to groundwater. The

  19. Phospholipid Fatty Acids as Physiological Indicators of Paracoccus denitrificans Encapsulated in Silica Sol-Gel Hydrogels

    Directory of Open Access Journals (Sweden)

    Josef Trögl

    2015-02-01

    Full Text Available The phospholipid fatty acid (PLFA content was determined in samples of Paracoccus denitrificans encapsulated in silica hydrogel films prepared from prepolymerized tetramethoxysilane (TMOS. Immediately after encapsulation the total PLFA concentration was linearly proportional to the optical density (600 nm of the input microbial suspension (R2 = 0.99. After 7 days this relationship remained linear, but with significantly decreased slope, indicating a higher extinction of bacteria in suspensions of input concentration 108 cells/mL and higher. trans-Fatty acids, indicators of cytoplasmatic membrane disturbances, were below the detection limit. The cy/pre ratio (i.e., ratio of cyclopropylated fatty acids (cy17:0 + cy19:0 to their metabolic precursors (16:1ω7 + 18:1ω7, an indicator of the transition of the culture to a stationary growth-phase, decreased depending on co-immobilization of nutrients in the order phosphate buffer > mineral medium > Luria Broth rich medium. The ratio, too, was logarithmically proportional to cell concentration. These results confirm the applicability of total PLFA as an indicator for the determination of living biomass and cy/pre ratio for determination of nutrient limitation of microorganisms encapsulated in sol-gel matrices. This may be of interest for monitoring of sol-gel encapsulated bacteria proposed as optical recognition elements in biosensor construction, as well as other biotechnological applications.

  20. Effects of Citric and Lactic Acid on the Reduction of Deoxynivalenol and Its Derivatives in Feeds

    Science.gov (United States)

    Humer, Elke; Lucke, Annegret; Harder, Hauke; Metzler-Zebeli, Barbara U.; Böhm, Josef; Zebeli, Qendrim

    2016-01-01

    Exposure to mycotoxin-contaminated feeds represents a serious health risk. This has necessitated the need for the establishment of practical methods for mycotoxin decontamination. This study investigated the effects of citric acid (CA) and lactic acid (LA) on common trichothecene mycotoxins in feeds contaminated with Fusarium mycotoxins. Contaminated feed samples were processed either with 5% CA or 5% LA solutions in a ratio of 1:1.2 (w/v) for 5, 24, or 48 h, and analyzed for multiple mycotoxin metabolites using a liquid chromatography–tandem mass spectrometric method. The analyses showed that treating the feed with CA and LA lowered the concentration of deoxynivalenol (DON), whereby 5% LA lowered the original DON concentration in the contaminated feed samples by half, irrespective of the processing time. Similar lowering effects were observed for the concentrations of 15Ac-DON, 5-hydroxyculmorin, and sambucinol. The concentration of nivalenol was only lowered by the LA treatment. In contrast, CA and LA treatments showed no or only small effects on the concentration of several mycotoxins and their derivatives, including zearalenone, fumonisins, and culmorin. In conclusion, the present results indicate that the use of 5% solutions of LA and CA might reduce the concentration of common trichothecene mycotoxins, especially DON and its derivate 15Ac-DON. However, further research is required to determine the effect on overall toxicity and to identify the underlying mechanisms. PMID:27690101

  1. Synthesis and Application of Phenyl Nitrone Derivatives as Acidic and Microbial Corrosion Inhibitors

    Directory of Open Access Journals (Sweden)

    Shijun Chen

    2015-01-01

    Full Text Available Nitrone has drawn great attention due to its wide applications as a 1,3-dipole in heterocyclic compounds synthesis and the bioactivities. With the special structure, nitrone can also be used as ligand in inorganic chemistry. Based on the current research, the nitrones are anticipated to be effective inhibitors against acidic and microbial corrosion. The aim of this work is to investigate the inhibitory action of nitrones. In this work, a series of phenyl nitrone derivatives (PN was synthesized and used as acidic and microbial corrosion inhibitors. The results indicate that several compounds show moderate to high inhibition efficiency (IE in 3% HCl. Accompanied with HMTA or BOZ, the IEs greatly increase, and the highest efficiency of 98.5% was obtained by using PN4 + BOZ. Investigation of the antibacterial activity against oilfield microorganism shows that the nitrone derivatives can inhibit SRB, IB, and TGB with moderate to high efficiency under 1,000 mg/L, which makes them potential to be used as bifunctional oilfield chemicals.

  2. Identification of the structure and origin of a thioacidolysis marker compound for ferulic acid incorporation into angiosperm lignins (and an indicator for cinnamoyl CoA reductase deficiency).

    Science.gov (United States)

    Ralph, John; Kim, Hoon; Lu, Fachuang; Grabber, John H; Leplé, Jean-Charles; Berrio-Sierra, Jimmy; Derikvand, Mohammad Mir; Jouanin, Lise; Boerjan, Wout; Lapierre, Catherine

    2008-01-01

    A molecular marker compound, derived from lignin by the thioacidolysis degradative method, for structures produced when ferulic acid is incorporated into lignin in angiosperms (poplar, Arabidopsis, tobacco), has been structurally identified as 1,2,2-trithioethyl ethylguaiacol [1-(4-hydroxy-3-methoxyphenyl)-1,2,2-tris(ethylthio)ethane]. Its truncated side chain and distinctive oxidation state suggest that it derives from ferulic acid that has undergone bis-8-O-4 (cross) coupling during lignification, as validated by model studies. A diagnostic contour for such structures is found in two-dimensional (13)C-(1)H correlated (HSQC) NMR spectra of lignins isolated from cinnamoyl CoA reductase (CCR)-deficient poplar. As low levels of the marker are also released from normal (i.e. non-transgenic) plants in which ferulic acid may be present during lignification, notably in grasses, the marker is only an indicator for CCR deficiency in general, but is a reliable marker in woody angiosperms such as poplar. Its derivation, together with evidence for 4-O-etherified ferulic acid, strongly implies that ferulic acid is incorporated into angiosperm lignins. Its endwise radical coupling reactions suggest that ferulic acid should be considered an authentic lignin precursor. Moreover, ferulic acid incorporation provides a new mechanism for producing branch points in the polymer. The findings sharply contradict those reported in a recent study on CCR-deficient Arabidopsis.

  3. Synthesis and pharmacology of N-alkylated derivatives of the excitotoxin ibotenic acid

    DEFF Research Database (Denmark)

    Madsen, U; Dumpis, M A; Bräuner-Osborne, Hans

    1998-01-01

    Three amino-alkylated derivatives of the naturally occurring excitatory amino acid (EAA) receptor agonist ibotenic acid (Ibo) have been synthesized and tested pharmacologically. N-Methyl-Ibo (1a) and N-ethyl-Ibo (1b) were shown to be agonists at NMDA receptors (EC50 = 140 and 320 microM, respecti......Three amino-alkylated derivatives of the naturally occurring excitatory amino acid (EAA) receptor agonist ibotenic acid (Ibo) have been synthesized and tested pharmacologically. N-Methyl-Ibo (1a) and N-ethyl-Ibo (1b) were shown to be agonists at NMDA receptors (EC50 = 140 and 320 micro...

  4. Pseudoephedrine-Directed Asymmetric α-Arylation of α-Amino Acid Derivatives.

    Science.gov (United States)

    Atkinson, Rachel C; Fernández-Nieto, Fernando; Mas Roselló, Josep; Clayden, Jonathan

    2015-07-27

    Available α-amino acids undergo arylation at their α position in an enantioselective manner on treatment with base of N'-aryl urea derivatives ligated to pseudoephedrine as a chiral auxiliary. In situ silylation and enolization induces diastereoselective migration of the N'-aryl group to the α position of the amino acid, followed by ring closure to a hydantoin with concomitant explulsion of the recyclable auxiliary. The hydrolysis of the hydantoin products provides derivatives of quaternary amino acids. The arylation avoids the use of heavy-metal additives, and is successful with a range of amino acids and with aryl rings of varying electronic character.

  5. New insights into the electrochemical behavior of acid orange 7: Convergent paired electrochemical synthesis of new aminonaphthol derivatives

    Science.gov (United States)

    Momeni, Shima; Nematollahi, Davood

    2017-02-01

    Electrochemical behavior of acid orange 7 has been exhaustively studied in aqueous solutions with different pH values, using cyclic voltammetry and constant current coulometry. This study has provided new insights into the mechanistic details, pH dependence and intermediate structure of both electrochemical oxidation and reduction of acid orange 7. Surprisingly, the results indicate that a same redox couple (1-iminonaphthalen-2(1H)-one/1-aminonaphthalen-2-ol) is formed from both oxidation and reduction of acid orange 7. Also, an additional purpose of this work is electrochemical synthesis of three new derivatives of 1-amino-4-(phenylsulfonyl)naphthalen-2-ol (3a–3c) under constant current electrolysis via electrochemical oxidation (and reduction) of acid orange 7 in the presence of arylsulfinic acids as nucleophiles. The results indicate that the electrogenerated 1-iminonaphthalen-2(1 H)-one participates in Michael addition reaction with arylsulfinic acids to form the 1-amino-3-(phenylsulfonyl)naphthalen-2-ol derivatives. The synthesis was carried out in an undivided cell equipped with carbon rods as an anode and cathode.

  6. Synthesis and Anti-tumor Activity of Novel Amide Derivatives of Ursolic Acid

    Institute of Scientific and Technical Information of China (English)

    2008-01-01

    Ursolic acid was modified at C3 and C28 position to obtain fourteen derivatives including twelve novel compounds, and their chemical structures were characterized by IR, 1H NMR and MS. Cell growth inhibitory effects of the derivatives against Hela cell were evaluated by MTT assay. All these derivatives were found to have stronger cell growth inhibitory than their parent compound, ursolic acid. The derivatives with a substituted acetyl group at C3hydroxyl group show better activities than those with an unsubstituted hydroxyl group.

  7. Endothelial Differentiation of Human Adipose-Derived Stem Cells on Polyglycolic Acid/Polylactic Acid Mesh

    Directory of Open Access Journals (Sweden)

    Meng Deng

    2015-01-01

    Full Text Available Adipose-derived stem cell (ADSC is considered as a cell source potentially useful for angiogenesis in tissue engineering and regenerative medicine. This study investigated the growth and endothelial differentiation of human ADSCs on polyglycolic acid/polylactic acid (PGA/PLA mesh compared to 2D plastic. Cell adhesion, viability, and distribution of hADSCs on PGA/PLA mesh were observed by CM-Dil labeling, live/dead staining, and SEM examination while endothelial differentiation was evaluated by flow cytometry, Ac-LDL/UEA-1 uptake assay, immunofluorescence stainings, and gene expression analysis of endothelial related markers. Results showed hADSCs gained a mature endothelial phenotype with a positive ratio of 21.4 ± 3.7% for CD31+/CD34− when induced in 3D mesh after 21 days, which was further verified by the expressions of a comprehensive range of endothelial related markers, whereas hADSCs in 2D induced and 2D/3D noninduced groups all failed to differentiate into endothelial cells. Moreover, compared to 2D groups, the expression for α-SMA was markedly suppressed in 3D cultured hADSCs. This study first demonstrated the endothelial differentiation of hADSCs on the PGA/PLA mesh and pointed out the synergistic effect of PGA/PLA 3D culture and growth factors on the acquisition of mature characteristic endothelial phenotype. We believed this study would be the initial step towards the generation of prevascularized tissue engineered constructs.

  8. Total nitrogen vs. amino-acid profile as indicator of protein content of beef.

    Science.gov (United States)

    Hall, Nicolette G; Schönfeldt, Hettie C

    2013-10-01

    In most cited food composition studies and tables, the proximate system measures protein as total nitrogen (N) (determined by Kjeldahl or Dumas method) multiplied by a specific factor. A factor of 6.25 is used for determining total protein from total N (Jones, Munsey, & Walker, 1942). Although more expensive, it is considered more accurate to base protein content of foods on amino acid data (Greenfield & Southgate, 2003). A study on the nutrient composition of beef analysed the full amino-acid profile of fifteen retail cuts from three age groups and six fat codes, as well as determined total nitrogen content to determine proximate protein composition. For all cuts, the correlation coefficient of total amino acids to protein (N×6.25) was 0.635. This indicates a poor correlation for predicting actual protein content (as determined by total amino acid count), based on the nitrogen factor of 6.25. On average, the sum of amino acids per cut amounted to 91% of total determined protein (N×6.25) for the same cut.

  9. Phenolic acid metabolites as biomarkers for tea- and coffee-derived polyphenol exposure in human subjects.

    Science.gov (United States)

    Hodgson, Jonathan M; Chan, Shin Yee; Puddey, Ian B; Devine, Amanda; Wattanapenpaiboon, Naiyana; Wahlqvist, Mark L; Lukito, Widjaja; Burke, Valerie; Ward, Natalie C; Prince, Richard L; Croft, Kevin D

    2004-02-01

    Tea and coffee are rich in polyphenols with a variety of biological activities. Many of the demonstrated activities are consistent with favourable effects on the risk of chronic diseases. 4-O-methylgallic acid (4OMGA) and isoferulic acid are potential biomarkers of exposure to polyphenols derived from tea and coffee respectively. 4OMGA is derived from gallic acid in tea, and isoferulic acid is derived from chlorogenic acid in coffee. Our major objective was to explore the relationships of tea and coffee intake with 24 h urinary excretion of 4OMGA and isoferulic acid in human subjects. The relationships of long-term usual (111 participants) and contemporaneously recorded current (344 participants) tea and coffee intake with 24 h urinary excretion of 4OMGA and isoferulic acid were assessed in two populations. 4OMGA was related to usual (r 0.50, Pcoffee intake. Overall, our present results are consistent with the proposal that 4OMGA is a good biomarker for black tea-derived polyphenol exposure, but isoferulic acid may be of limited usefulness as a biomarker for coffee-derived polyphenol exposure.

  10. Agar media that indicate acid production from sorbitol by oral microorganisms.

    OpenAIRE

    Kalfas, S.; Edwardsson, S

    1985-01-01

    Two varieties of agar medium (Trypticase [BBL Microbiology Systems]-serum-sorbitol-bromcresol purple agar [TSSB] and Trypticase-blood-sorbitol-CaCO3 agar [TBSCa]) indicating microbial acid production from sorbitol were tested. The media were devised for use in studies on the prevalence of sorbitol-fermenting human oral microorganisms incubated in an anaerobic or microaerophilic atmosphere containing 5 to 6% CO2. TSSB contains bromcresol purple as the pH indicator and NaHCO3 as the main buffer...

  11. Spectroscopic studies on the interaction of cinnamic acid and its hydroxyl derivatives with human serum albumin

    Science.gov (United States)

    Min, Jiang; Meng-Xia, Xie; Dong, Zheng; Yuan, Liu; Xiao-Yu, Li; Xing, Chen

    2004-04-01

    Cinnamic acid and its derivatives possess various biological effects in remedy of many diseases. Interaction of cinnamic acid and its hydroxyl derivatives, p-coumaric acid and caffeic acid, with human serum albumin (HSA), and concomitant changes in its conformation were studied using fluorescence and Fourier transform infrared spectroscopic methods. Fluorescence data revealed the presence of one binding site on HSA for cinnamic acid and its hydroxyl derivatives, and their binding constants ( KA) are caffeic acid> p-coumaric acid> cinnamic acid when Cdrug/ CHSA ranging from 1 to 10. The changes of the secondary structure of HSA after interacting with the three drugs are estimated, respectively by combining the curve-fitting results of amid I and amid III bands. The α-helix structure has a decrease of ≈9, 5 and 3% after HSA interacted with caffeic acid, p-coumaric acid and cinnamic acid, respectively. It was found that the hydroxyls substituted on aromatic ring of the drugs play an important role in the changes of protein's secondary structure. Combining the result of fluorescence quenching and the changes of secondary structure of HSA after interaction with the three drugs, the drug-HSA interaction mode was discussed.

  12. Cellular fatty acid composition of marine-derived fungi

    Digital Repository Service at National Institute of Oceanography (India)

    PrabhaDevi; Shridhar, M.P.D.; DeSouza, L.; Naik, C.G.

    ) and eicosapentanoeic acid (EPA) are recognized to have beneficial influence on human health 11,12 and is included in various infant foods as DHA. DHA is considered to be particularly important in infant nutrition and brain development 13, 14 . The main source...

  13. Stereoselective synthesis of amino acid derivatives using carbohydrates as templates

    OpenAIRE

    Kunz, Horst; Sager, Wilfried; Pfrengle, Waldemar; Laschat, Sabine; Schanzenbach, Dirk

    1993-01-01

    Glycosylamines contain the easily cleavable semi-aminal-type N-glycosidic bond. O-Protected glycosylamines, therefore, can advantageously be used as a form of "asymmetric ammonia", for instance, in Strecker syntheses and in Ugi reactions to give amino acid amides as well as in modifications of the Mannich reaction.

  14. Breakdown kinetics of C-hydroxymethyl beta-dicarbonyl derivatives of carbon acids: implications in the bioconversion rate of C-phosphoryloxymethyl prodrugs of carbon acids.

    Science.gov (United States)

    Dhareshwar, Sundeep S; Stella, Valentino J

    2009-05-01

    The kinetics of conversion of C-hydroxymethyl derivatives of pharmaceutically relevant beta-dicarbonyl carbon acids of two series, pyrazolidin-3,5-diones and inden-1,3-diones, and a model carbon acid back to the respective carbon acids were studied as a function of pH at 25 degrees C and an ionic strength of 0.15 M. This is a somewhat surprising reaction since it involves the facile breakdown of a carbon-carbon bond. The slopes of the pH-rate profiles for the dehydroxymethylation were approximately unity, which along with the lack of buffer catalysis, indicates a specific-base mechanism involving spontaneous breakdown of the oxymethyl anion. This breakdown generates the conjugate base of the respective carbon acids. Thus within a series, there exists a correlation between the second-order rate constant for dehydroxymethylation and the pK(a) of the corresponding carbon acid with a shorter conversion/dehydroxymethylation half-life (at all given pH values) with decreasing pK(a) of the parent carbon acid. The increasing acidity of the carbon acid affords an increase in the leaving group ability of the carbanion, and therefore facilitation of the rate-determining unimolecular carbon-carbon bond cleavage. Since the hydroxymethyl derivative is an intermediate in the bioconversion of C-phosphoryloxymethyl prodrugs of carbon acids, also under study, the relationship allows one to reasonably predict how facile the dehydroxymethylation would be for any new beta-dicarbonyl carbon acid.

  15. Retinoic acid derived from the fetal ovary initiates meiosis in mouse germ cells.

    Science.gov (United States)

    Mu, Xinyi; Wen, Jing; Guo, Meng; Wang, Jianwei; Li, Ge; Wang, Zhengpin; Wang, Yijing; Teng, Zhen; Cui, Yan; Xia, Guoliang

    2013-03-01

    Meiotic initiation of germ cells at 13.5 dpc (days post-coitus) indicates female sex determination in mice. Recent studies reveal that mesonephroi-derived retinoic acid (RA) is the key signal for induction of meiosis. However, whether the mesonephroi is dispensable for meiosis is unclear and the role of the ovary in this meiotic process remains to be clarified. This study provides data that RA derived from fetal ovaries is sufficient to induce germ cell meiosis in a fetal ovary culture system. When fetal ovaries were collected from 11.5 to 13.5 dpc fetuses, isolated and cultured in vitro, germ cells enter meiosis in the absence of mesonephroi. To exclude RA sourcing from mesonephroi, 11.5 dpc urogenital ridges (UGRs; mesonephroi and ovary complexes) were treated with diethylaminobenzaldehyde (DEAB) to block retinaldehyde dehydrogenase (RALDH) activity in the mesonephros and the ovary. Meiosis occurred when DEAB was withdrawn and the mesonephros was removed 2 days later. Furthermore, RALDH1, rather than RALDH2, serves as the major RA synthetase in UGRs from 12.5 to 15.5 dpc. DEAB treatment to the ovary alone was able to block germ cell meiotic entry. We also found that exogenously supplied RA dose-dependently reduced germ cell numbers in ovaries by accelerating the entry into meiosis. These results suggest that ovary-derived RA is responsible for meiosis initiation.

  16. An efficient synthesis of 1,5-benzodiazepine derivatives catalyzed by boric acid

    Institute of Scientific and Technical Information of China (English)

    Xin Zhou; Mei Yue Zhang; Shu Tao Gao; Jing Jun Ma; Chun Wang; Chao Liu

    2009-01-01

    1,5-Benzodiazepine derivatives have been synthesized by the condensation of o-phenylenediamines and ketones in the presence of boric acid as catalyst under mild conditions. This method is simple, environmentally benign and high yielding.

  17. PRENYLATED BENZOIC ACID DERIVATIVES FROM PIPER SPECIES AS SOURCE OF ANTI-INFECTIVE AGENTS

    OpenAIRE

    2012-01-01

    A number of prenylated benzoic acids derivatives with interesting biological activities have been previously isolated and characterized from different species of piperaceae family. Several Piper species contained structurally similar compounds with diverse biological activities such as anti-bacterial, anti-fungal, insecticidal as well as anti-parasitic all of which produces compounds that can be classified as prenylated benzoic acid derivatives. Piper sp has proven to serve as a source of pot...

  18. Amino acid size, charge, hydropathy indices and matrices for protein structure analysis

    Directory of Open Access Journals (Sweden)

    Biro JC

    2006-03-01

    Full Text Available Abstract Background Prediction of protein folding and specific interactions from only the sequence (ab initio is a major challenge in bioinformatics. It is believed that such prediction will prove possible if Anfinsen's thermodynamic principle is correct for all kinds of proteins, and all the information necessary to form a concrete 3D structure is indeed present in the sequence. Results We indexed the 200 possible amino acid pairs for their compatibility regarding the three major physicochemical properties – size, charge and hydrophobicity – and constructed Size, Charge and Hydropathy Compatibility Indices and Matrices (SCI & SCM, CCI & CCM, and HCI & HCM. Each index characterized the expected strength of interaction (compatibility of two amino acids by numbers from 1 (not compatible to 20 (highly compatible. We found statistically significant positive correlations between these indices and the propensity for amino acid co-locations in real protein structures (a sample containing total 34630 co-locations in 80 different protein structures: for HCI: p We tried to predict or reconstruct simple 2D representations of 3D structures from the sequence using these matrices by applying a dot plot-like method. The location and pattern of the most compatible subsequences was very similar or identical when the three fundamentally different matrices were used, which indicates the consistency of physicochemical compatibility. However, it was not sufficient to choose one preferred configuration between the many possible predicted options. Conclusion Indexing of amino acids for major physico-chemical properties is a powerful approach to understanding and assisting protein design. However, it is probably insufficient itself for complete ab initio structure prediction.

  19. Silica with immobilized phosphinic acid-derivative for uranium extraction.

    Science.gov (United States)

    Budnyak, Tetyana M; Strizhak, Alexander V; Gładysz-Płaska, Agnieszka; Sternik, Dariusz; Komarov, Igor V; Kołodyńska, Dorota; Majdan, Marek; Tertykh, Valentin А

    2016-08-15

    A novel adsorbent benzoimidazol-2-yl-phenylphosphinic acid/aminosilica adsorbent (BImPhP(O)(OH)/SiO2NH2) was prepared by carbonyldiimidazole-mediated coupling of aminosilica with 1-carboxymethylbenzoimidazol-2-yl-phenylphosphinic acid. It was obtained through direct phosphorylation of 1-cyanomethylbenzoimidazole by phenylphosphonic dichloride followed by basic hydrolysis of the nitrile. The obtained sorbent was well characterized by physicochemical methods, such as differential scanning calorimetry-mass spectrometry (DSC-MS), surface area and pore distribution analysis (ASAP), scanning electron microscopy (SEM), X-ray photoelectron (XPS) and Fourier transform infrared (FTIR) spectroscopies. The adsorption behavior of the sorbent and initial silica gel as well as aminosilica gel with respect to uranium(VI) from the aqueous media has been studied under varying operating conditions of pH, concentration of uranium(VI), contact time, and desorption in different media. The synthesized material was found to show an increase in adsorption activity with respect to uranyl ions in comparison with the initial compounds. In particular, the highest adsorption capacity for the obtained modified silica was found at the neutral pH, where one gram of the adsorbent can extract 176mg of uranium. Under the same conditions the aminosilica extracts 166mg/g, and the silica - 144mg/g of uranium. In the acidic medium, which is common for uranium nuclear wastes, the synthesized adsorbent extracts 27mg/g, the aminosilica - 16mg/g, and the silica - 14mg/g of uranium. It was found that 15% of uranium ions leached from the prepared material in acidic solutions, while 4% of uranium can be removed in a phosphate solution.

  20. Agar media that indicate acid production from sorbitol by oral microorganisms.

    Science.gov (United States)

    Kalfas, S; Edwardsson, S

    1985-12-01

    Two varieties of agar medium (Trypticase [BBL Microbiology Systems]-serum-sorbitol-bromcresol purple agar [TSSB] and Trypticase-blood-sorbitol-CaCO3 agar [TBSCa]) indicating microbial acid production from sorbitol were tested. The media were devised for use in studies on the prevalence of sorbitol-fermenting human oral microorganisms incubated in an anaerobic or microaerophilic atmosphere containing 5 to 6% CO2. TSSB contains bromcresol purple as the pH indicator and NaHCO3 as the main buffering salt. TBSCa contains CaCO3 as both the buffering salt and the indicator of acid production. The growth yield of pure cultures of oral microorganisms on TBSCa was shown to equal that on blood agar incubated under similar conditions. TSSB inhibited the growth of several bacteria to various extents. The recovery of sorbitol-fermenting microorganisms from oral specimens was the greatest when the specimens were assayed with TBSCa. The poorer results obtained with TSSB were mainly due to the decoloration of the pH indicator in this medium and the presence of greater numbers of sorbitol false-positive colonies.

  1. Stability-indicating methods for the determination of erdosteine in the presence of its acid degradation products.

    Science.gov (United States)

    Moustafa, Nadia M; Badawey, Amr M; Lamie, Nesrine T; El-Aleem, Abd El-Aziz B Abd

    2014-01-01

    Four accurate, sensitive, and reproducible stability-indicating methods for the determination of erdosteine in the presence of its acid degradation products are presented. The first method involves processing the spectra by using a first-derivative method at 229 nm in a concentration range of 10-70 microg/mL. The mean percentage recovery was 100.43 +/- 0.977. The second method is based on ratio-spectra first derivative spectrophotometry at 227.4 and 255 nm over a concentration range of 10-70 microg/mL. The mean percentage recovery was 99.65 +/- 1.122% and 100.02 +/- 1.306% at 227.4 and 255 nm, respectively. The third method utilizes quantitative densitometric evaluation of the TLC of erdosteine in the presence of its acid degradation products, and uses methanol-chloroform-ammonia (7 + 3 +/- 0.01, v/v/v) as the mobile phase. TLC chromatograms were scanned at 235 nm. This method analyzes erdosteine in a concentration range of 2.4-5.6 microg/spot, with a mean percentage recovery of 100.03 +/- 1.015%. The fourth method is HPLC for the simultaneous determination of erdosteine in the presence of its acid degradation products. The mobile phase consists of water-methanol (65 + 35, v/v). The standard curve of erdosteine showed good linearity over a concentration range of 10-80 microg/mL, with a mean percentage recovery of 99.90 +/- 1.207%. These methods were successfully applied to the determination of erdosteine in bulk powder, laboratory-prepared mixtures containing different percentages of the degradation products, and pharmaceutical dosage forms. The validity of results was assessed by applying the standard addition technique. The results obtained agreed statistically with those obtained by a reported method, showing no significant differences with respect to accuracy and precision.

  2. Lysine requirements of pre-lay broiler breeder pullets: determination by indicator amino acid oxidation.

    Science.gov (United States)

    Coleman, Russell A; Bertolo, Robert F; Moehn, Soenke; Leslie, Michael A; Ball, Ronald O; Korver, Doug R

    2003-09-01

    The indicator amino acid oxidation (IAAO) method allows the determination of amino acid requirements under conditions of low growth rate as found in pre-laying broiler breeder pullets. Cobb 500 breeder pullets (20 wk old; 2290 +/- 280 g, n = 4) were adapted (6 d) to a pelleted, purified control diet containing all nutrients at >or=110% of NRC recommendations. After recovery from surgery for implantation of a jugular catheter, each bird was fed, in random order, test diets containing one of nine levels of lysine (0.48, 0.96, 1.92, 2.88, 3.84, 4.80, 7.68, 9.60 and 14.40 g/kg of diet). Indicator oxidation was determined during 4-h primed (74 kBq/kg body), constant infusions (44 kBq x h(-1). kg body(-1)) of L-[1-(14)C]phenylalanine. Using the breakpoint of a one-slope broken-line model, the lysine requirement was determined to be 4.88 +/- 0.96 g/kg of diet or 366 +/- 72 mg x hen(-1) x d(-1) with an upper 95% CI of 6.40 g/kg of diet or 480 mg x hen(-1) x d(-1). IAAO allows determination of individual bird amino acid requirements for specific ages and types of birds over short periods of time and enables more accurate broiler breeder pullet diet formulation.

  3. Omega-3 fatty acid effects on biochemical indices following cancer surgery.

    Science.gov (United States)

    Stehr, Sebastian N; Heller, Axel R

    2006-11-01

    Epidemiological studies have indicated that a high intake of saturated fat and/or animal fat increases the risk of colon and breast cancer. Laboratory and clinical investigations have shown a reduced risk of colon carcinogenesis after alimentation with omega-3 fatty acids, as found in fish oil. Mechanisms accounting for these anti-tumor effects are reduced levels of PGE(2) and inducible NO synthase as well as an increased lipid peroxidation, or translation inhibition with subsequent cell cycle arrest. Further, omega-3 eicosapentaenoic acid is capable of down-regulating the production and effect of a number of mediators of cachexia, such as IL-1, IL-6, TNF-alpha and proteolysis-inducing factor. In patients with advanced cancer, it is possible to increase energy and protein intake via an enteral or parenteral route, but this seems to have little impact on progressive weight loss. Fish oil administration improved patients' conditions in cancer cachexia and during radio- and chemotherapy. In patients undergoing tumor resection surgery we observed improvement of liver and pancreas biochemical indices when omega-3 fatty acids were administered. This paper is a review of recent developments in the field of nutrition in cancer patients with emphasis on the acute phase response following cancer surgery and the beneficial aspects of fish oil administration.

  4. Simultaneous determination of acetylsalicylic and salicylic acids by first derivative spectrometry in pharmaceutical preparations

    Science.gov (United States)

    Rogić, Dunja

    1993-03-01

    A multicomponent first derivative UV spectrometric procedure for determination of acetylsalicylic acid (aspirin) and salicylic acid in the solution containing 1 % (w/v) of citric acid in some pharmaceutical preparations is presented. The method is based on the use of the first derivative minimum spectrometric measurements at 286 nm for aspirin and at 318 nm for salicylic acid. Four kinds of cmmercial Aspirin tablets were assayed without a long pretreatment of the pharmaceuticals from the tablet additives. Beer's law is obeyed from 13.62-68.1 μg ml -1 of aspirin and from 2.723-13.616 μg ml -1 of salicylic acid. Detection limits at the 0.05 level of significance were calculated to be 1.24 and 0.25 μg ml -1 with relative standard deviations of 1.09 % and 1.2 % of aspirin and salicylic acid, respectively.

  5. An Efficient Solid Acid Promoted Synthesis of Quinoxaline Derivatives at Room Temperature

    Institute of Scientific and Technical Information of China (English)

    AHMAD,Shaabani; ALI,Maleki

    2007-01-01

    Quinoxaline derivatives have been synthesized in a very short time with excellent yields by the condensation of 1,2-diamines with aliphatic or aromatic 1,2-dicarbonyl compounds or benzilmonoxime in the presence of silica sul-furic acid as a very inexpensive solid acid catalyst at room temperature. The recovery and reuse of the catalyst are also satisfactory.

  6. Mass spectral analysis of C3 and C4 aliphatic amino acid derivatives.

    Science.gov (United States)

    Lawless, J. G.; Chadha, M. S.

    1971-01-01

    Diagnostic criteria are obtained for the distinction of alpha, beta, gamma, and N-methyl isomers of the C3 and C4 aliphatic amino acids, using mass spectral analysis of the derivatives of these acids. The use of deuterium labeling has helped in the understanding of certain fragmentation pathways.

  7. No-solvent Condensation Reaction of Amino Acids and their Derivatives with Pyrandione

    Institute of Scientific and Technical Information of China (English)

    2001-01-01

    Synthesis of a novel series of N-pyrandione substituted amino acids and their esters 3 via a condensation reaction between pyrandione and amino acid or their derivatives in excess ethyl orthoformate without solvent is described. The stereochemistry of 3 has been discussed.

  8. Chiral BINOL-derived phosphoric acids: privileged Brønsted acid organocatalysts for C-C bond formation reactions.

    Science.gov (United States)

    Zamfir, Alexandru; Schenker, Sebastian; Freund, Matthias; Tsogoeva, Svetlana B

    2010-12-07

    BINOL-derived phosphoric acids have emerged during the last five years as powerful chiral Brønsted acid catalysts in many enantioselective processes. The most successful transformations carried out with chiral BINOL phosphates include C-C bond formation reactions. The recent advances have been reviewed in this article with a focus being placed on hydrocyanations, aldol-type, Mannich, Friedel-Crafts, aza-ene-type, Diels-Alder, as well as cascade and multi-component reactions.

  9. A novel trans-4-hydroxycinnamic acid derivative from Meyer lemon (Citrus meyeri).

    Science.gov (United States)

    Miyake, Yoshiaki; Ito, Chihiro; Itoigawa, Masataka

    2012-12-15

    Isolation and structural elucidation of a new trans-4-hydroxycinnamic acid derivative from Meyer lemon (Citrus meyeri hort. ex Y. Tanaka) was carried out. The derivative exhibited the antioxidative activity by ORAC (oxygen radical absorbance capacity) assay and was found in the flavedo and alvedo of Meyer lemon peel.

  10. Angular sensitivity of vegetation indices derived from CHRIS/PROBA data

    NARCIS (Netherlands)

    Verrelst, J.; Schaepman, M.E.; Kötz, B.; Kneubühler, M.

    2008-01-01

    View angle effects present in spectral vegetation indices can either be regarded as an added source of uncertainty for variable retrieval or as a source of additional information, enhancing the variable retrieval; however, the magnitude of these angular effects remains for most indices unknown or un

  11. Satellite derived integrated water vapor and rain intensity patterns - Indicators of rapid cyclogenesis

    Science.gov (United States)

    Mcmurdie, Lynn; Katsaros, Kristina

    1992-01-01

    We examine integrated water vapor fields and rain intensity patterns derived from the Scanning Multichannel Microwave Radiometer (SMMR) and Special Sensor Microwave/Imager (SSM/I) for several rapidly deepening and non-rapidly deepening midlatitude cyclones in the North Atlantic. Our goal is to identify features in the satellite data unique to the rapidly deepening cases, and to explore how these data can potentially be used in the analysis and forecasting of these events.

  12. Satellite derived integrated water vapor and rain intensity patterns: Indicators of rapid cyclogenesis

    Science.gov (United States)

    Mcmurdie, Lynn; Katsaros, Kristina

    1992-01-01

    We examine integrated water vapor fields and rain intensity patterns derived from the Scanning Multichannel Microwave Radiometer (SMMR) and Special Sensor Microwave/Imager (SSM/I) for several rapidly deepening and non-rapidly deepening midlatitude cyclones in the North Atlantic. Our goal is to identify features in the satellite data unique to the rapidly deepening cases, and to explore how these data can potentially be used in the analysis and forecasting of these events.

  13. Two New Cholic Acid Derivatives from the Marine Ascidian-Associated Bacterium Hasllibacter halocynthiae

    Directory of Open Access Journals (Sweden)

    Sung Hun Kim

    2012-10-01

    Full Text Available The investigation of secondary metabolites in liquid cultures of a recently discovered marine bacterium, Hasllibacter halocynthiae strain KME 002T, led to the isolation of two new cholic acid derivatives. The structures of these compounds were determined to be 3,3,12-trihydroxy-7-ketocholanic acid (1 and 3,3,12-trihydroxy-7-deoxycholanic acid (2 through HRFABMS and NMR data analyses.

  14. Metabolic engineering for microbial production of aromatic amino acids and derived compounds.

    Science.gov (United States)

    Bongaerts, J; Krämer, M; Müller, U; Raeven, L; Wubbolts, M

    2001-10-01

    Metabolic engineering to design and construct microorganisms suitable for the production of aromatic amino acids and derivatives thereof requires control of a complicated network of metabolic reactions that partly act in parallel and frequently are in rapid equilibrium. Engineering the regulatory circuits, the uptake of carbon, the glycolytic pathway, the pentose phosphate pathway, and the common aromatic amino acid pathway as well as amino acid importers and exporters that have all been targeted to effect higher productivities of these compounds are discussed.

  15. Modification of oligo-Ricinoleic Acid and Its Derivatives with 10-Undecenoic Acid via Lipase-Catalyzed Esterification

    Directory of Open Access Journals (Sweden)

    M. Claudia Montiel

    2012-04-01

    Full Text Available Lipases were employed under solvent-free conditions to conjugate oligo-ricinoleic acid derivatives with 10-undecenoic acid, to incorporate a reactive terminal double bond into the resultant product. First, undecenoic acid was covalently attached to oligo-ricinoleic acid using immobilized Candida antarctica lipase (CAL at a 30% yield. Thirty percent conversion also occurred for CAL-catalyzed esterification between undecenoic acid and biocatalytically-prepared polyglycerol polyricinoleate (PGPR, with attachment of undecenoic acid occurring primarily at free hydroxyls of the polyglycerol moiety. The synthesis of oligo-ricinoleyl-, undecenoyl- structured triacylglycerols comprised two steps. The first step, the 1,3-selective lipase-catalyzed interesterification of castor oil with undecenoic acid, occurred successfully. The second step, the CAL-catalyzed reaction between ricinoleyl-, undecenoyl structured TAG and ricinoleic acid, yielded approximately 10% of the desired structured triacylglycerols (TAG; however, a significant portion of the ricinoleic acid underwent self-polymerization as a side-reaction. The employment of gel permeation chromatography, normal phase HPLC, NMR, and acid value measurements was effective for characterizing the reaction pathways and products that formed.

  16. Indicator-based and indicator-free magnetic assays connected with disposable electrochemical nucleic acid sensor system.

    Science.gov (United States)

    Karadeniz, Hakan; Erdem, Arzum; Kuralay, Filiz; Jelen, Frantisek

    2009-04-15

    An indicator-based and indicator-free magnetic assays connected with a disposable pencil graphite electrode (PGE) were successfully developed, and also compared for the electrochemical detection of DNA hybridization. The oxidation signals of echinomycin (ECHI) and electroactive DNA bases, guanine and adenine, respectively were monitored in the presence of DNA hybridization by using differential pulse voltammetry (DPV) technique. The biotinylated probe was immobilized onto the magnetic beads (magnetic particles, microspheres) and hybridization with its complementary target at the surface of particles within the medium was exhibited successfully using electrochemical sensor system. For the selectivity studies, the results represent that both indicator-based and indicator-free magnetic assays provide a better discrimination for DNA hybridization compared to duplex with one-base or more mismatches. The detection limits (S/N=3) of the magnetic assays based on indicator or indicator-free were found in nM concentration level of target using disposable sensor technology with good reproducibility. The characterization and advantages of both proposed magnetic assays connected with a disposable electrochemical sensor are also discussed and compared with those methods previously reported in the literature.

  17. Synthesis and Bioactivity of (R)-Ricinoleic Acid Derivatives: A Review.

    Science.gov (United States)

    Pabiś, Sylwia; Kula, Józef

    2016-01-01

    (R)-Ricinoleic acid (RA) [(12R,9Z)-hydroxyoctadecenoic acid], the main compound of castor seed oil, because of its unusual structure readily undergoes multi-directional chemical and biochemical transformations to produce derivatives with the retained carbon skeleton or with its degradation. Many of these are of high biological activity, as documented by an in vitro study, and possess therapeutic potential. This review article provides an overview of the recent developments in the area of synthesis of RA based compounds with anticancer and antimicrobial activities. Moreover, the antiinflammatory and analgesic properties of some ricinoleic acid derivatives are also highlighted.

  18. Photosensitization of Nanocrystalline TiO2 Electrode Modifiedwith C60 Carboxylic Acid Derivatives

    Institute of Scientific and Technical Information of China (English)

    张文; 史亚茹; 甘良兵; 黄春辉; 王艳琴; 虎民

    2001-01-01

    C60 carboxylic acid derivatives can be readily adsorbed on the surface of nanocrystalline TiO2 films act as charge-transfer sensitizer. The electron transport from TiO2 to the C60 derivatives results in the generation of the cathodic photocurrent. The short-circuit photocurrent of a C60 tetracarboxylic acid is 0.45 μA/cm2 under 464 um light illumination. The photoelectric behaviour of ITO electrodes modified by the same C60 carboxylic acids is different from that of the modified TiO2 electrodes, and shows anodic photocurrent.

  19. Derivation of indices of socioeconomic status for health services research in Asia

    Directory of Open Access Journals (Sweden)

    Arul Earnest

    2015-01-01

    Conclusion: These indices may prove useful for policy-makers to identify spatially varying risk factors, and in turn help identify geographically targeted intervention programs, which can be more cost effective to conduct.

  20. Decay resistance of wood treated with boric acid and tall oil derivates.

    Science.gov (United States)

    Temiz, Ali; Alfredsen, Gry; Eikenes, Morten; Terziev, Nasko

    2008-05-01

    In this study, the effect of two boric acid concentrations (1% and 2%) and four derivates of tall oil with varying chemical composition were tested separately and in combination. The tall oil derivates were chosen in a way that they consist of different amounts of free fatty, resin acids and neutral compounds. Decay tests using two brown rot fungi (Postia placenta and Coniophora puteana) were performed on both unleached and leached test samples. Boric acid showed a low weight loss in test samples when exposed to fungal decay before leaching, but no effect after leaching. The tall oil derivates gave better efficacy against decay fungi compared to control, but are not within the range of the efficacy needed for a wood preservative. Double impregnation with boric acid and tall oil derivates gave synergistic effects for several of the double treatments both in unleached and leached samples. In the unleached samples the double treatment gave a better efficacy against decay fungi than tall oil alone. In leached samples a better efficacy against brown rot fungi were achieved than in samples with boron alone and a nearly similar or better efficacy than for tall oil alone. Boric acid at 2% concentration combined with the tall oil derivate consisting of 90% free resin acids (TO-III) showed the best performance against the two decay fungi with a weight loss less than 3% after a modified pure culture test.

  1. Conversion of α-linolenic acid to long-chain omega-3 fatty acid derivatives and alterations of HDL density subfractions and plasma lipids with dietary polyunsaturated fatty acids in Monk parrots (Myiopsitta monachus).

    Science.gov (United States)

    Petzinger, C; Larner, C; Heatley, J J; Bailey, C A; MacFarlane, R D; Bauer, J E

    2014-04-01

    The effect of α-linolenic acid from a flaxseed (FLX)-enriched diet on plasma lipid and fatty acid metabolism and possible atherosclerosis risk factors was studied in Monk parrots (Myiopsitta monachus). Twenty-four Monk parrots were randomly assigned to diets containing either 10% ground SUNs or 10% ground FLXs. Feed intake was calculated daily. Blood samples, body condition scores and body weights were obtained at -5 weeks, day 0, 7, 14, 28, 42 and 70. Plasma samples were analysed for total cholesterol, free cholesterol, triacylglycerols and lipoproteins. Phospholipid subfraction fatty acid profiles were determined. By day 70, the FLX group had significantly higher plasma phospholipid fatty acids including 18:3n-3 (α-linolenic acid), 20:5n-3 (eicosapentaenoic acid) and 22:6n-3 (docosahexaenoic acid). The sunflower group had significantly higher plasma phospholipid levels of 20:4n-6 (arachidonic acid). By day 70, the high-density lipoprotein (HDL) peak shifted resulting in significantly different HDL peak densities between the two experimental groups (1.097 g/ml FLX group and 1.095 g/ml SUN group, p = 0.028). The plasma fatty acid results indicate that Monk parrots can readily convert α-linolenic acid to the long-chain omega-3 derivatives including docosahexaenoic acid and reduce 20:4n-6 accumulation in plasma phospholipids. The reason for a shift in the HDL peak density is unknown at this time.

  2. Metabolic Engineering of Yeast to Produce Fatty Acid-derived Biofuels: Bottlenecks and Solutions

    Directory of Open Access Journals (Sweden)

    Jiayuan eSheng

    2015-06-01

    Full Text Available Fatty acid-derived biofuels can be a better solution than bioethanol to replace petroleum fuel, since they have similar energy content and combustion properties as current transportation fuels. The environmentally friendly microbial fermentation process has been used to synthesize advanced biofuels from renewable feedstock. Due to their robustness as well as the high tolerance to fermentation inhibitors and phage contamination, yeast strains such as Saccharomyces cerevisiae and Yarrowia lipolytica have attracted tremendous attention in recent studies regarding the production of fatty acid-derived biofuels, including fatty acids, fatty acid ethyl esters, fatty alcohols, and fatty alkanes. However, the native yeast strains cannot produce fatty acids and fatty acid-derived biofuels in large quantities. To this end, we have summarized recent publications in this review on metabolic engineering of yeast strains to improve the production of fatty acid-derived biofuels, identified the bottlenecks that limit the productivity of biofuels, and categorized the appropriate approaches to overcome these obstacles.

  3. Synthesis, structure, and biological applications of α-fluorinated β-amino acids and derivatives.

    Science.gov (United States)

    March, Taryn L; Johnston, Martin R; Duggan, Peter J; Gardiner, James

    2012-11-01

    This review gives a broad overview of the state of play with respect to the synthesis, conformational properties, and biological activity of α-fluorinated β-amino acids and derivatives. General methods are described for the preparation of monosubstituted α-fluoro-β-amino acids (Scheme 1). Nucleophilic methods for the introduction of fluorine predominantly involve the reaction of DAST with alcohols derived from α-amino acids, whereas electrophilic sources of fluorine such as NFSI have been used in conjunction with Arndt-Eistert homologation, conjugate addition or organocatalyzed Mannich reactions. α,α-Difluoro-β-amino acids have also been prepared using DAST; however, this area of synthesis is largely dominated by the use of difluorinated Reformatsky reagents to introduce the difluoro ester functionality (Scheme 9). α-Fluoro-β-amino acids and derivatives analyzed by X-ray crystal and NMR solution techniques are found to adopt preferred conformations which are thought to result from stereoelectronic effects associated with F located close to amines, amides, and esters (Figs. 2-6). α-Fluoro amide and β-fluoro ethylamide/amine effects can influence the secondary structure of α-fluoro-β-amino acid-containing derivatives including peptides and peptidomimetics (Figs. 7-9). α-Fluoro-β-amino acids are also components of a diverse range of bioactive anticancer (e.g., 5-fluorouracil), antifungal, and antiinsomnia agents as well as protease inhibitors where such fluorinated analogs have shown increased potency and spectrum of activity.

  4. Identification and quantitation of new glutamic acid derivatives in soy sauce by UPLC/MS/MS.

    Science.gov (United States)

    Frerot, Eric; Chen, Ting

    2013-10-01

    Glutamic acid is an abundant amino acid that lends a characteristic umami taste to foods. In fermented foods, glutamic acid can be found as a free amino acid formed by proteolysis or as a non-proteolytic derivative formed by microorganisms. The aim of the present study was to identify different structures of glutamic acid derivatives in a typical fermented protein-based food product, soy sauce. An acidic fraction was prepared with anion-exchange solid-phase extraction (SPE) and analyzed by UPLC/MS/MS and UPLC/TOF-MS. α-Glutamyl, γ-glutamyl, and pyroglutamyl dipeptides, as well as lactoyl amino acids, were identified in the acidic fraction of soy sauce. They were chemically synthesized for confirmation of their occurrence and quantified in the selected reaction monitoring (SRM) mode. Pyroglutamyl dipeptides accounted for 770 mg/kg of soy sauce, followed by lactoyl amino acids (135 mg/kg) and γ-glutamyl dipeptides (70 mg/kg). In addition, N-succinoylglutamic acid was identified for the first time in food as a minor compound in soy sauce (5 mg/kg).

  5. New hydroxamic acid derivatives of fluoroquinolones: synthesis and evaluation of antibacterial and anticancer properties.

    Science.gov (United States)

    Rajulu, Gavara Govinda; Bhojya Naik, Halehatty Seephya; Viswanadhan, Abhilash; Thiruvengadam, Jayaraman; Rajesh, Kondodiyil; Ganesh, Sambasivam; Jagadheshan, Hiriyan; Kesavan, Poonimangadu Koppolu

    2014-01-01

    A series of new hydroxamic acid derivatives (6a-f) at C-3 position of fluoroquinolones were designed and synthesized through multistep synthesis. The design concept involved replacement of the 3-carboxylic acid in fluoquinolones with hydroxamic acid as an acid mimicking group. The synthetic work employed in this work provides a good example for the synthesis of pure hydroxamic acid based fluoroquinolones. The synthesized compounds were characterized by (1)H-NMR, electrospray ionization (ESI)-MS and IR. The new compounds were tested for their in vitro antimicrobial and anti-proliferative activity. Out of the six derivatives, compound 6e exhibited moderate antibacterial activity by inhibiting the growth of Escherichia coli and Klebsiella pneumoniae (MIC: 4.00-8.00 µg/mL). Compounds 6b and 6f displayed good growth inhibition against A549 Lung adenocarcinoma and HCT-116 Colon carcinoma cell lines.

  6. Effect of the structure of gallic acid and its derivatives on their interaction with plant ferritin.

    Science.gov (United States)

    Wang, Qunqun; Zhou, Kai; Ning, Yong; Zhao, Guanghua

    2016-12-15

    Gallic acid and its derivatives co-exist with protein components in foodstuffs, but there is few report on their interaction with proteins. On the other hand, plant ferritin represents not only a novel class of iron supplement, but also a new nanocarrier for encapsulation of bioactive nutrients. However, plant ferritin is easy to be degraded by pepsin in the stomach, thereby limiting its application. Herein, we investigated the interaction of gallic acid and its derivatives with recombinant soybean seed H-2 ferritin (rH-2). We found that these phenolic acids interacted with rH-2 in a structure-dependent manner; namely, gallic acid (GA), methyl gallate (MEGA) and propyl gallate (PG) having three HO groups can bind to rH-2, while their analogues with two HO groups cannot. Consequently, such binding largely inhibited ferritin degradation by pepsin. These findings advance our understanding of the relationship between the structure and function of phenolic acids.

  7. Comparison of pH-sensitive degradability of maleic acid amide derivatives.

    Science.gov (United States)

    Kang, Sunyoung; Kim, Youngeun; Song, Youngjun; Choi, Jin Uk; Park, Euddeum; Choi, Wonmin; Park, Jeongseon; Lee, Yan

    2014-05-15

    We synthesized five maleic acid amide derivatives (maleic, citraconic, cis-aconitic, 2-(2'-carboxyethyl) maleic, 1-methyl-2-(2'-carboxyethyl) maleic acid amide), and compared their degradability for the future development of pH-sensitive biomaterials with tailored kinetics of the release of drugs, the change of charge density, and the degradation of scaffolds. The degradation kinetics was highly dependent upon the substituents on the cis-double bond. Among the maleic acid amide derivatives, 2-(2'-carboxyethyl) maleic acid amide with one carboxyethyl and one hydrogen substituent showed appropriate degradability at weakly acidic pH, and the additional carboxyl group can be used as a pH-sensitive linker.

  8. Microbial production of amino acids and derived chemicals: synthetic biology approaches to strain development.

    Science.gov (United States)

    Wendisch, Volker F

    2014-12-01

    Amino acids are produced at the multi-million-ton-scale with fermentative production of l-glutamate and l-lysine alone being estimated to amount to more than five million tons in the year 2013. Metabolic engineering constantly improves productivities of amino acid producing strains, mainly Corynebacterium glutamicum and Escherichia coli strains. Classical mutagenesis and screening have been accelerated by combination with intracellular metabolite sensing. Synthetic biology approaches have allowed access to new carbon sources to realize a flexible feedstock concept. Moreover, new pathways for amino acid production as well as fermentative production of non-native compounds derived from amino acids or their metabolic precursors were developed. These include dipeptides, α,ω-diamines, α,ω-diacids, keto acids, acetylated amino acids and ω-amino acids.

  9. Synthesis, characterization, and computational study of the supramolecular arrangement of a novel cinnamic acid derivative.

    Science.gov (United States)

    Oliveira, S S; Santin, L G; Almeida, L R; Malaspina, L A; Lariucci, C; Silva, J F; Fernandes, W B; Aquino, G L B; Gargano, R; Camargo, A J; Napolitano, H B

    2017-02-01

    In this work, we present the synthesis, characterization, and computational study of the supramolecular arrangement of a new cinnamic acid derivative: ethyl-(2E)-3-(4-hydroxy-3,5-dimethoxyphenyl)-prop-2-enoate (EHD). Single crystals of EHD were obtained using ethyl ether as solvent and a slow evaporation technique. Its crystallographic structure, derived from X-ray diffraction experiments, includes a disordered water molecule on the EHD supramolecular structure. This water molecule participates in four O-H···O hydrogen bonds, which are arranged as a centrosymmetric H-bond array with the water at the center. Electronic and structural properties of the isolated EHD molecule and of the EHD molecule in the presence of one water molecule were calculated at the B3LYP/6-311++G(2d,2p) level of theory. These calculations show that the HOMO-LUMO energy gap of EHD decreases upon the introduction of the water molecule, suggesting that EHD becomes a stronger electron acceptor. These results indicate that the water molecule helps to stabilize the crystal structure in this system containing unequal numbers of acceptor and donor atoms. The supramolecular synthon involving the disordered water molecule and the supramolecular features presented here provide new possibilities in the design of functional materials and should also help us to gain a deeper understanding of the processes by which molecules recognize biological targets.

  10. Bioconversion of volatile fatty acids derived from waste activated sludge into lipids by Cryptococcus curvatus.

    Science.gov (United States)

    Liu, Jia; Liu, Jia-Nan; Yuan, Ming; Shen, Zi-Heng; Peng, Kai-Ming; Lu, Li-Jun; Huang, Xiang-Feng

    2016-07-01

    Pure volatile fatty acid (VFA) solution derived from waste activated sludge (WAS) was used to produce microbial lipids as culture medium in this study, which aimed to realize the resource recovery of WAS and provide low-cost feedstock for biodiesel production simultaneously. Cryptococcus curvatus was selected among three oleaginous yeast to produce lipids with VFAs derived from WAS. In batch cultivation, lipid contents increased from 10.2% to 16.8% when carbon to nitrogen ratio increased from about 3.5 to 165 after removal of ammonia nitrogen by struvite precipitation. The lipid content further increased to 39.6% and the biomass increased from 1.56g/L to 4.53g/L after cultivation for five cycles using sequencing batch culture (SBC) strategy. The lipids produced from WAS-derived VFA solution contained nearly 50% of monounsaturated fatty acids, including palmitic acid, heptadecanoic acid, ginkgolic acid, stearic acid, oleic acid, and linoleic acid, which showed the adequacy of biodiesel production.

  11. Effect of Different Omega-6/Omega-3 Polyunsaturated Fatty Acid Ratios on the Formation of Monohydroxylated Fatty Acids in THP-1 Derived Macrophages

    Directory of Open Access Journals (Sweden)

    Kathrin Keeren

    2015-04-01

    Full Text Available Omega-6 and omega-3 polyunsaturated fatty acids (n-6 and n-3 PUFA can modulate inflammatory processes. In western diets, the content of n-6 PUFA is much higher than that of n-3 PUFA, which has been suggested to promote a pro-inflammatory phenotype. The aim of this study was to analyze the effect of modulating the n-6/n-3 PUFA ratio on the formation of monohydroxylated fatty acid (HO-FAs derived from the n-6 PUFA arachidonic acid (AA and the n-3 PUFAs eicosapentaenoic acid (EPA and docosahexaenoic acid (DHA in THP-1 macrophages by means of LC-MS. Lipid metabolites were measured in THP-1 macrophage cell pellets. The concentration of AA-derived hydroxyeicosatetraenoic acids (HETEs was not significantly changed when incubated THP-1 macrophages in a high AA/(EPA+DHA ratio of 19/1 vs. a low ratio AA/(EPA+DHA of 1/1 (950.6 ± 110 ng/mg vs. 648.2 ± 92.4 ng/mg, p = 0.103. Correspondingly, the concentration of EPA-derived hydroxyeicosapentaenoic acids (HEPEs and DHA-derived hydroxydocosahexaenoic acids (HDHAs were significantly increased (63.9 ± 7.8 ng/mg vs. 434.4 ± 84.3 ng/mg, p = 0.012 and 84.9 ± 18.3 ng/mg vs. 439.4 ± 82.7 ng/mg, p = 0.014, respectively. Most notable was the strong increase of 18-hydroxyeicosapentaenoic acid (18-HEPE formation in THP-1 macrophages, with levels of 170.9 ± 40.2 ng/mg protein in the high n-3 PUFA treated cells. Thus our data indicate that THP-1 macrophages prominently utilize EPA and DHA for monohydroxylated metabolite formation, in particular 18-HEPE, which has been shown to be released by macrophages to prevent pressure overload-induced maladaptive cardiac remodeling.

  12. Evaluation of the Protein Requirement in Chinese Young Adults Using the Indicator Amino Acid Oxidation Technique

    Institute of Scientific and Technical Information of China (English)

    LI Min; ZHANG Yu Hui; WANG Zhi Ling; GOU Ling Yan; LI Wei Dong; TIAN Yuan; HU Yi Chun; WANG Rui; PIAO Jian Hua; YANG Xiao Guang

    2013-01-01

    Objective To accurately calculate the protein requirements in Chinese young adults using the indicator amino acid oxidation technique. Methods Nine women and ten men received a restricted daily level of protein intake (0.75, 0.82, 0.89, 0.97, and 1.05 g/kg), along with L-[1-13C]-leucine. Subjects’ protein requirement was determined by a biphasic linear regression crossover analysis of F13CO2 data. In doing so, a breakpoint at the minimal rate of appearance of 13CO2 expiration specific to each level of dietary protein was identified. This trial was registered with the Chinese clinical trial registry as ChiCTR-ONC-11001407. Results The Estimated Average Requirement (EAR) and the Recommended Nutrient Intake (RNI) of protein for healthy Chinese young adults were determined to be 0.87 and 0.98 g/(kg·d), respectively, based on the indicator amino acid oxidation technique. Conclusion The EAR and RNI of mixed protein are 5% and 16% that are lower than the current proposed EAR and RNI (0.92 and 1.16 g/(kg·d), respectively), as determined by the nitrogen balance method. The respective EAR and RNI recommendations of 0.87 and 0.98 g/(kg·d) of mixed protein are estimated to be reasonable and suitable for Chinese young adults.

  13. Evaluation of the diagnostic performance of platelet-derived indices for the differential diagnosis of thrombocytopenia in pediatrics

    Directory of Open Access Journals (Sweden)

    Nelson Hernando Aponte-Barrios

    2014-10-01

    Full Text Available Background. Platelet-derived indices have a well-established correlation with the differential diagnosis of thrombocytopenia in adult-based research. These indices include mean platelet volume, platelet distribution width, and platelet-large cell ratio. Objective. To determine the values of platelet-derived indices in a pediatric population with diagnoses of thrombocytopenia and their etiologic correlation. Materials and methods. Analytic observational diagnostic-test study. The population for this analytical study was pediatric patients between 6 months and 18 years of age who had thrombocytopenia (<100x10(9/L. The study period was 18 months long. Results. Of 54 subjects, 18 (33.3% were diagnosed with idiopathic thrombocytopenic purpura, and 36 (66.7% were diagnosed with acute leukemia. Mean age was 7.4 years and 6.8 years for immune thrombocytopenic purpura and acute leukemia, respectively. Mean platelet distribution width values for immune thrombocytopenic purpura and acute leukemia were 15.08 fL and 10.73, respectively. Mean MPV for immune thrombocytopenic purpura and acute leukemia was 11.7 fL and 9.8 fL, respectively. Mean platelet-large cell ratio was 38.26% and 24.97% for idiopathic thrombocytopenic purpura and acute leukemia, respectively. Differences in these three distinct platelet indices between idiopathic thrombocytopenic purpura and acute leukemia were statistically significant (p=0.00. The area under the ROC curve for platelet-derived indices showed that they were adequate for defining the causes of thrombocytopenia. MPV and platelet-large cell ratio had an area under the curve of 0.89 and 0.88, respectively, while platelet size deviation width had an area under the curve of 0.903. Conclusions. Platelet-derived indices could be useful in the initial approach for the differential diagnosis of pediatric patients with thrombocytopenia.

  14. Improving surface functional properties of tofu whey-derived peptides by chemical modification with fatty acids.

    Science.gov (United States)

    Matemu, Athanasia Oswald; Katayama, Shigeru; Kayahara, Hisataka; Murasawa, Hisashi; Nakamura, Soichiro

    2012-04-01

    Effect of acylation with saturated fatty acids on surface functional properties of tofu whey-derived peptides was investigated. Tofu whey (TW) and soy proteins (7S, 11S, and acid-precipitated soy protein [APP]) were hydrolyzed by Protease M 'Amano' G, and resulting peptide mixtures were acylated with esterified fatty acids of different chain length (6C to 18C) to form a covalent linkage between the carboxyl group of fatty acid and the free amino groups of peptide. Acylation significantly (P whey ultra filtered fraction (UFTW proteins.

  15. Usage of Smartphone Data to Derive an Indicator for Collaborative Mobility between Individuals

    Directory of Open Access Journals (Sweden)

    Bogdan Toader

    2017-02-01

    Full Text Available Thepotentialofgeospatialbigdatahasbeendrawingattentionfor afewyears. Despitethe larger and larger market penetration of portable technologies (nomadic and wearable devices like smartphones and smartwatches, their opportunities for travel behavior analysis are still relatively unexplored. The main objective of our study is to extract the human mobility patterns from GPS tracesin order toderivean indicatorfor enhancing CollaborativeMobility (CM betweenindividuals. The first step, extracting activity duration and location, is done using state-of-the-art automated recognition tools. Sensors data are used to reconstruct individual’s activity location and duration across time. For constructing the indicator, in a second step, we defined different variables and methods for specific case studies. Smartphone sensor data are being collected from a limited number of individuals and for one week. These data are used to evaluate the proposed indicator. Based on the value of the indicator, we analyzed the potential for identifying CM among groups of users, such as sharing traveling resources (e.g., carpooling, ridesharing, parking sharing and time (rescheduling and reordering activities.

  16. Appraisal of active tectonics in Hindu Kush: Insights from DEM derived geomorphic indices and drainage analysis

    Directory of Open Access Journals (Sweden)

    Syed Amer Mahmood

    2012-07-01

    The results obtained from these indices were combined to yield an index of relative active tectonics (IRAT using GIS. The average of the seven measured geomorphic indices was used to evaluate the distribution of relative tectonic activity in the study area. We defined four classes to define the degree of relative tectonic activity: class 1__very high (1.0 ≤ IRAT < 1.3; class 2__high (1.3 ≥ IRAT < 1.5; class 3—moderate (1.5 ≥ IRAT < 1.8; and class 4—low (1.8 ≥ IRAT. In view of the results, we conclude that this combined approach allows the identification of the highly deformed areas related to active tectonics. Landsat imagery and field observations also evidence the presence of active tectonics based on the deflected streams, deformed landforms, active mountain fronts and triangular facets. The indicative values of IRAT are consistent with the areas of known relative uplift rates, landforms and geology.

  17. Cinnamic Acid and Its Derivatives: Mechanisms for Prevention and Management of Diabetes and Its Complications

    Science.gov (United States)

    Adisakwattana, Sirichai

    2017-01-01

    With recent insight into the development of dietary supplements and functional foods, search of effective phytochemical compounds and their mechanisms involved in prevention and management of diabetes and its complications are now being assessed. Cinnamic acid and its derivatives occur naturally in high levels of plant-based foods. Among various biological activities, cinnamic acid and its derivatives are associated with a beneficial influence on diabetes and its complications. The aim of the review is to summarize the potential mechanisms of these compounds for prevention and management of diabetes and its complications. Based on several in vitro studies and animal models, cinnamic acid and its derivatives act on different mechanism of actions, including stimulation of insulin secretion, improvement of pancreatic β-cell functionality, inhibition of hepatic gluconeogenesis, enhanced glucose uptake, increased insulin signaling pathway, delay of carbohydrate digestion and glucose absorption, and inhibition of protein glycation and insulin fibrillation. However, due to the limited intestinal absorption being a result of low bioavailability of cinnamic acid and its derivatives, current improvement efforts with entrapping into solid and liquid particles are highlighted. Further human clinical studies are needed to clarify the effects of cinnamic acid and its derivatives in diabetic patients. PMID:28230764

  18. Design and synthesis of Quinazolinone, Benzothiazole derivatives bearing guanidinopropanoic acid moiety and their Schiff bases as cytotoxic and antimicrobial agents

    Directory of Open Access Journals (Sweden)

    Palani Venkatesh

    2016-09-01

    Full Text Available Two series of Benzothiazole, Quinazolinone derivatives bearing guanidinopropanoic acid (38 compounds including 27 intermediates and one series of Schiff base derivatives (14 compounds were synthesized, characterized then evaluated for their cytotoxicity against human cervix cell line (HeLa by MTT assay; antimicrobial activity against 11 pathogenic bacteria, 10 pathogenic fungus using standard of ciprofloxacin and Clotrimazole respectively. Compounds 13–18 showed significant activity against HeLa with IC50 range of 2–550 μM. Compound 3-(3-(6-hydroxybenzo[d]thiazol-2-ylguanidinopropanoic acid (18 showed potent activity against human HeLa cell line with the half maximal inhibitory concentration (IC50 values of 1.8 μM which was close to the value of the positive control, doxorubicin. Antimicrobial result indicated that, compounds showed differential activity against the tested fungus and bacteria. Compounds 11, 14, 38 and 49 exhibited potent antibacterial and antifungal activity.

  19. Boronic acid-tethered amphiphilic hyaluronic acid derivative-based nanoassemblies for tumor targeting and penetration.

    Science.gov (United States)

    Jeong, Jae Young; Hong, Eun-Hye; Lee, Song Yi; Lee, Jae-Young; Song, Jae-Hyoung; Ko, Seung-Hak; Shim, Jae-Seong; Choe, Sunghwa; Kim, Dae-Duk; Ko, Hyun-Jeong; Cho, Hyun-Jong

    2017-02-16

    (3-Aminomethylphenyl)boronic acid (AMPB)-installed hyaluronic acid-ceramide (HACE)-based nanoparticles (NPs), including manassantin B (MB), were fabricated for tumor-targeted delivery. The amine group of AMPB was conjugated to the carboxylic acid group of hyaluronic acid (HA) via amide bond formation, and synthesis was confirmed by spectroscopic methods. HACE-AMPB/MB NPs with a 239-nm mean diameter, narrow size distribution, negative zeta potential, and >90% drug encapsulation efficiency were fabricated. Exposed AMPB in the outer surface of HACE-AMPB NPs (in the aqueous environment) may react with sialic acid of cancer cells. The improved cellular accumulation efficiency, in vitro antitumor efficacy, and tumor penetration efficiency of HACE-AMPB/MB NPs, compared with HACE/MB NPs, in MDA-MB-231 cells (CD44 receptor-positive human breast adenocarcinoma cells) may be based on the CD44 receptor-mediated endocytosis and phenylboronic acid-sialic acid interaction. Enhanced in vivo tumor targetability, infiltration efficiency, and antitumor efficacies of HACE-AMPB NPs, compared with HACE NPs, were observed in a MDA-MB-231 tumor-xenografted mouse model. In addition to passive tumor targeting (based on an enhanced permeability and retention effect) and active tumor targeting (interaction between HA and CD44 receptor), the phenylboronic acid-sialic acid interaction can play important roles in augmented tumor targeting and penetration of HACE-AMPB NPs. STATEMENT OF SIGNIFICANCE: (3-Aminomethylphenyl)boronic acid (AMPB)-tethered hyaluronic acid-ceramide (HACE)-based nanoparticles (NPs), including manassantin B (MB), were fabricated and their tumor targeting and penetration efficiencies were assessed in MDA-MB-231 (CD44 receptor-positive human adenocarcinoma) tumor models. MB, which exhibited antitumor efficacies via the inhibition of angiogenesis and hypoxia inducible factor (HIF)-1, was entrapped in HACE-AMPB NPs in this study. Phenylboronic acid located in the outer surface

  20. Structure–anticancer activity relationships among 4-azolidinone-3-carboxylic acids derivatives

    Directory of Open Access Journals (Sweden)

    Lesyk R. B.

    2010-04-01

    Full Text Available The aim of present research was investigation of anticancer activity of 4-azolidinone-3-carboxylic acids derivatives, and studies of structure–activity relationships (SAR aspects. Methods. Organic synthesis; spectral methods; anticancer screening was performed according to the US NCI protocol (Developmental Therapeutic Program. Results. The data of new 4-thiazolidinone-3-alkanecarboxylic acids derivatives in vitro anticancer activity were described. The most active compounds which belong to 5-arylidene-2,4- thia(imidazolidinone-3-alkanecarboxylic acids; 5-aryl(heterylidenerhodanine-3-succinic acids derivatives were selected. Determination of some SAR aspects which allowed to determine directions in lead- compounds structure optimization, as well as desirable molecular fragments for design of potential anticancer agents based on 4-azolidinone scaffold were performed. 5-Arylidenehydantoin-3-acetic acids amides were identified as a new class of significant selective antileukemic agents. Possible pharmacophore scaffold of 5-ylidenerhodanine-3-succinic acids derivatives was suggested. Conclusions. The series of active compounds with high anticancer activity and/or selectivity levels were selected. Some SAR aspects were determined and structure design directions were proposed.

  1. Aqueous solubility study of salts of benzylamine derivatives and p-substituted benzoic acid derivatives using X-ray crystallographic analysis

    DEFF Research Database (Denmark)

    Parshad, Henrik; Frydenvang, Karla Andrea; Liljefors, Tommy;

    2004-01-01

    than those reported for the corresponding salts of benzylamine (I). Thermal analysis indicated that the increased solubility was caused by reduced crystal lattice energy, which was most likely due to the reduced number of strong hydrogen bonds of the salt of (II) and (III). X-ray crystallographic...... analysis of p-hydroxybenzoic acid salt of (I), (II) and (III) suggested that the reduced number of hydrogen bonds caused the apparent higher solubility. Further analyses of seven salts of (I) were performed. It was not possible to identify any relationship between the number of hydrogen bonds......Twenty two p-substituted benzoic acid derivates were used to prepare salts of N-methylbenzylamine (II) and N,N-dimethylbenzylamine (III), respectively. Only five salts of (II) and two salts of (III) were obtained in a crystalline state. The solubility of these salts was orders of magnitude higher...

  2. A digital image-based method for determining of total acidity in red wines using acid-base titration without indicator.

    Science.gov (United States)

    Tôrres, Adamastor Rodrigues; Lyra, Wellington da Silva; de Andrade, Stéfani Iury Evangelista; Andrade, Renato Allan Navarro; da Silva, Edvan Cirino; Araújo, Mário César Ugulino; Gaião, Edvaldo da Nóbrega

    2011-05-15

    This work proposes the use of digital image-based method for determination of total acidity in red wines by means of acid-base titration without using an external indicator or any pre-treatment of the sample. Digital images present the colour of the emergent radiation which is complementary to the radiation absorbed by anthocyanines present in wines. Anthocyanines change colour depending on the pH of the medium, and from the variation of colour in the images obtained during titration, the end point can be localized with accuracy and precision. RGB-based values were employed to build titration curves, and end points were localized by second derivative curves. The official method recommends potentiometric titration with a NaOH standard solution, and sample dilution until the pH reaches 8.2-8.4. In order to illustrate the feasibility of the proposed method, titrations of ten red wines were carried out. Results were compared with the reference method, and no statistically significant difference was observed between the results by applying the paired t-test at the 95% confidence level. The proposed method yielded more precise results than the official method. This is due to the trivariate nature of the measurements (RGB), associated with digital images.

  3. The relationship between satellite-derived indices and species diversity across African savanna ecosystems

    Science.gov (United States)

    Mapfumo, Ratidzo B.; Murwira, Amon; Masocha, Mhosisi; Andriani, R.

    2016-10-01

    The ability to use remotely sensed diversity is important for the management of ecosystems at large spatial extents. However, to achieve this, there is still need to develop robust methods and approaches that enable large-scale mapping of species diversity. In this study, we tested the relationship between species diversity measured in situ with the Normalized Difference Vegetation Index (NDVI) and the Coefficient of Variation in the NDVI (CVNDVI) derived from high and medium spatial resolution satellite data at dry, wet and coastal savanna woodlands. We further tested the effect of logging on NDVI along the transects and between transects as disturbance may be a mechanism driving the patterns observed. Overall, the results of this study suggest that high tree species diversity is associated with low and high NDVI and at intermediate levels is associated with low tree species diversity and NDVI. High tree species diversity is associated with high CVNDVI and vice versa and at intermediate levels is associated with high tree species diversity and CVNDVI.

  4. Theophylline-7-acetic acid derivatives with amino acids as anti-tuberculosis agents.

    Science.gov (United States)

    Voynikov, Yulian; Valcheva, Violeta; Momekov, Georgi; Peikov, Plamen; Stavrakov, Georgi

    2014-07-15

    A series of amides were synthesized by condensation of theophylline-7-acetic acid and eight commercially available amino acid methyl ester hydrochlorides. Consecutive hydrolysis of six of the amido-esters resulted in the formation of corresponding amido-acids. The newly synthesized compounds were evaluated for their in vitro activity against Mycobacterium tuberculosis H37Rv. The activity varied depending on the amino acid fragments and in seven cases exerted excellent values with MICs 0.46-0.26 μM. Assessment of the cytotoxicity revealed that the compounds were not cytotoxic against the human embryonal kidney cell line HEK-293T. The theophylline-7-acetamides containing amino acid moieties appear to be promising lead compounds for the development of antimycobacterial agents.

  5. An automated system for access to derived climate indices in support of ecological impacts assessments and resource management

    Science.gov (United States)

    Walker, J.; Morisette, J. T.; Talbert, C.; Blodgett, D. L.; Kunicki, T.

    2012-12-01

    A U.S. Geological Survey team is working with several providers to establish standard data services for the climate projection data they host. To meet the needs of climate adaptation science and landscape management communities, the team is establishing a set of climate index calculation algorithms that will consume data from various providers and provide directly useful data derivatives. Climate projections coming from various scenarios, modeling centers, and downscaling methods are increasing in number and size. Global change impact modeling and assessment, generally, requires inputs in the form of climate indices or values derived from raw climate projections. This requirement puts a large burden on a community not familiar with climate data formats, semantics, and processing techniques and requires storage capacity and computing resources out of the reach of most. In order to fully understand the implications of our best available climate projections, assessments must take into account an ensemble of climate projections and potentially a range of parameters for calculation of climate indices. These requirements around data access and processing are not unique from project to project, or even among projected climate data sets, pointing to the need for a reusable tool to generate climate indices. The U.S. Geological Survey has developed a pilot application and supporting web service framework that automates the generation of climate indices. The web service framework consists of standards-based data servers and a data integration broker. The resulting system allows data producers to publish and maintain ownership of their data and data consumers to access climate derivatives via a simple to use "data product ordering" workflow. Data access and processing is completed on enterprise "cloud" computing resources and only the relatively small, derived climate indices are delivered to the scientist or land manager. These services will assist the scientific and land

  6. Identification of marine-derived lipids in juvenile coho salmon and aquatic insects through fatty acid analysis

    Science.gov (United States)

    Heintz, Ron A.; Wipfli, Mark S.; Hudson, John P.

    2010-01-01

    The energetic benefits enjoyed by consumers in streams with salmon runs depend on how those benefits are accrued. Adult Pacific salmon Oncorhynchus spp. deliver significant amounts of nutrients (i.e., nitrogen and phosphorus) and carbon to streams when they spawn and die; these nutrient additions can have demonstrable effects on primary production in streams. Consumption of carcass tissues or eggs provides for direct energy subsidies to consumers and may have significant effects on their condition. In this study, comparisons of juvenile coho salmon O. kisutch and aquatic insects exposed to terrestrial and marine energy sources demonstrated that direct consumption of marine-derived lipids had a significant effect on the lipid reserves of consumers. Direct consumption of marine-derived tissues was verified through fatty acid analysis. Selected aquatic insects and juvenile coho salmon were reared for 6 weeks in experimental streams supplied with terrestrial or marine energy sources. Chironomid midges, nemourid stoneflies, and juvenile coho salmon exposed to the marine energy source altered their fatty acid compositions by incorporating the long-chain polyunsaturated fatty acids that are characteristic of marine fish. The fatty acid composition of baetid mayflies was unaffected. The direct movement of specific fatty markers indicated that direct consumption of marine-derived tissues led to increased energy reserves (triacylglycerols) in consumers. Similar results were obtained for juvenile coho salmon sampled from natural streams before and after the arrival of adult salmon runs. These data indicate that marine-derived lipids from anadromous fish runs are an important source of reserve lipids for consumers that overwinter in streams.

  7. New Biocompatible Polyesters Derived from α-Amino Acids: Hydrolytic Degradation Behavior

    Directory of Open Access Journals (Sweden)

    Jeoshua Katzhendler

    2010-10-01

    Full Text Available New polymers were synthesized from α-hydroxy acids derived from the natural amino acids Ile, Leu, Phe, and Val, combined with lactic acid, glycolic acid and 6-hydroxyhexanoic acid by direct condensation. The toxicity was determined and the degradation process of these polyesters was investigated under physiological conditions by analyzing the composition of the degraded polymers and the oligomers cleaved in the buffer medium. The polymers were found to be non toxic to two cell lines. Polymers displayed a biphasic degradation behavior. In most cases, a linear relationship was found between the weight loss constant and the hydrophobicity of the polymers, Log P. Regarding the second stage of weight loss, it is apparent that polymers derived from α-hydroxy(Lisoleucine ((LHOIle and α-hydroxy(LValine ((LHOVal degraded much faster than those derived from α-hydroxy(Lleucine ((LHOLeu and α-hydroxy(Lphenylalanine ((LHOPhe, probably due to different spatial orientation of the side chains. Copolymers of 6-hydroxyhexanoic acid displayed slow degradation rates as expected, whereas the degradation profile of copolymers of lactic acid was similar to the other homopolymers. These new polyesters may serve as potential biocompatible materials for medical applications.

  8. Solution properties and emulsification properties of amino acid-based gemini surfactants derived from cysteine.

    Science.gov (United States)

    Yoshimura, Tomokazu; Sakato, Ayako; Esumi, Kunio

    2013-01-01

    Amino acid-based anionic gemini surfactants (2C(n)diCys, where n represents an alkyl chain with a length of 10, 12, or 14 carbons and "di" and "Cys" indicate adipoyl and cysteine, respectively) were synthesized using the amino acid cysteine. Biodegradability, equilibrium surface tension, and dynamic light scattering were used to characterize the properties of gemini surfactants. Additionally, the effects of alkyl chain length, number of chains, and structure on these properties were evaluated by comparing previously reported gemini surfactants derived from cystine (2C(n)Cys) and monomeric surfactants (C(n)Cys). 2C(n)diCys shows relatively higher biodegradability than does C(n)Cys and previously reported sugar-based gemini surfactants. Both critical micelle concentration (CMC) and surface tension decrease when alkyl chain length is increased from 10 to 12, while a further increase in chain length to 14 results in increased CMC and surface tension. This indicates that long-chain gemini surfactants have a decreased aggregation tendency due to the steric hindrance of the bulky spacer as well as premicelle formation at concentrations below the CMC and are poorly packed at the air/water interface. Formation of micelles (measuring 2 to 5 nm in solution) from 2C(n)diCys shows no dependence on alkyl chain length. Further, shaking the mixtures of aqueous 2C(n)diCys surfactant solutions and squalane results in the formation of oil-in-water type emulsions. The highly stable emulsions are formed using 2C₁₂diCys or 2C₁₄diCys solution and squalane in a 1:1 or 2:1 volume ratio.

  9. CO2 Adsorption by para-Nitroaniline Sulfuric Acid-Derived Porous Carbon Foam

    Directory of Open Access Journals (Sweden)

    Enrico Andreoli

    2016-12-01

    Full Text Available The expansion product from the sulfuric acid dehydration of para-nitroaniline has been characterized and studied for CO2 adsorption. The X-ray photoelectron spectroscopy (XPS characterization of the foam indicates that both N and S contents (15 and 9 wt%, respectively are comparable to those separately reported for nitrogen- or sulfur-containing porous carbon materials. The analysis of the XPS signals of C1s, O1s, N1s, and S2p reveals the presence of a large number of functional groups and chemical species. The CO2 adsorption capacity of the foam is 7.9 wt% (1.79 mmol/g at 24.5 °C and 1 atm in 30 min, while the integral molar heat of adsorption is 113.6 kJ/mol, indicative of the fact that chemical reactions characteristic of amine sorbents are observed for this type of carbon foam. The kinetics of adsorption is of pseudo-first-order with an extrapolated activation energy of 18.3 kJ/mol comparable to that of amine-modified nanocarbons. The richness in functionalities of H2SO4-expanded foams represents a valuable and further pursuable approach to porous carbons alternative to KOH-derived activated carbons.

  10. PRENYLATED BENZOIC ACID DERIVATIVES FROM PIPER SPECIES AS SOURCE OF ANTI-INFECTIVE AGENTS

    Directory of Open Access Journals (Sweden)

    Ibrahim Malami

    2012-06-01

    Full Text Available A number of prenylated benzoic acids derivatives with interesting biological activities have been previously isolated and characterized from different species of piperaceae family. Several Piper species contained structurally similar compounds with diverse biological activities such as anti-bacterial, anti-fungal, insecticidal as well as anti-parasitic all of which produces compounds that can be classified as prenylated benzoic acid derivatives. Piper sp has proven to serve as a source of potential anti-infective agents by developing a biosynthetic route to the synthesis of prenylated benzoic acids derivative natural products as their chemical defense system. Despite the frequent isolation of these interesting compounds with strong biological activity, yet none have been taking into consideration for development into therapeutic agents.

  11. Antitrypanosomal Activity of Novel Benzaldehyde-Thiosemicarbazone Derivatives from Kaurenoic Acid

    Directory of Open Access Journals (Sweden)

    Cecília M. A. de Oliveira

    2011-01-01

    Full Text Available A series of new thiosemicarbazones derived from natural diterpene kaurenoic acid were synthesized and tested against the epimastigote forms of Trypanosoma cruzi to evaluate their antitrypanosomal potential. Seven of the synthesized thiosemicarbazones were more active than kaurenoic acid with IC50 values between 2-24.0 mM. The o-nitro-benzaldehyde-thiosemicarbazone derivative was the most active compound with IC50 of 2.0 mM. The results show that the structural modifications accomplished enhanced the antitrypanosomal activity of these compounds. Besides, the thiocyanate, thiosemicarbazide and the p- methyl, p-methoxy, p-dimethylamine, m-nitro and o-chlorobenzaldehyde-thiosemicarbazone derivatives displayed lower toxicity for LLMCK2 cells than kaurenoic acid, exhibing an IC50 of 59.5 mM.

  12. How much do different ways of calculating percentiles influence the derived performance indicators? - A case study

    CERN Document Server

    Schreiber, Michael

    2013-01-01

    Bibliometric indicators can be determined by comparing specific citation records with the percentiles of a reference set. However, there exists an ambiguity in the computation of percentiles because usually a significant number of papers with the same citation count are found at the border between percentile rank classes. The present case study of the citations to the journal Europhysics Letters (EPL) in comparison with all physics papers from the Web of Science shows the deviations which occur due to the different ways of treating the tied papers in the evaluation of the percentage of highly cited publications. A strong bias can occur, if the papers tied at the threshold number of citations are all considered as highly cited or all considered as not highly cited.

  13. BOOK REVIEW: Statistical & Financial – Accounting Statements and Systems Of Statistical Indicators Derived

    Directory of Open Access Journals (Sweden)

    Ion Iorga Simăn

    2014-03-01

    Full Text Available he type of management based on a complex system of indicators is now being applied as a logical and systematic approach to identifying, assessing, analyzing and communicating decisions, to enacting and monitoring the implementation of those decisions, being associated to any activity, function or business process in a way that enables organizations and companies to minimize the impact of threats and maximize opportunities. This type of management has been, and remains interdisciplinary and analytical in point of generating indicators, and finally it should treat all the activities in the organization or company in a holistic and synthetic manner. How much can a book, a course book, or a professor contribute to achieving such a vast and important goal, was the most difficult question throughout the process of writing book. We remembered, with a strange kind of joy, a passage from Leo Frobenius, dedicated to his own teachers, and we share it with our prospective readers for its sheer sincerity, freshness and candour: „From among the number of teachers I had during my years of education, two I will always keep in my memory… From the former (whose name did not even appear in the author’s account – n.m. I brought home a full notebook, in a clear and methodical style, and obtained an ordered system of knowledge, which would certainly have allowed me to pass any exam. Professor Heusler’s course of lectures failed to bring forth anything like this [… ]. On the contrary, after each of his classes I hurried back home in an infinitely elevated mood, full of creative impulses and the willingness to use the sharp weapons I had been given…”

  14. The Effects of Subacute Exposure of Peracetic Acid on Hematological Indices in Wistar Rats

    Directory of Open Access Journals (Sweden)

    Abbas Ali Keshtkar

    2008-01-01

    Full Text Available This study was done to determine the effects of subacute exposure of Peracetic acid on Hematological indices in Wistar rats. In this study 18 male Wistar rats divided to two experimental and one control groups. PAA with 99% purity purchased. Then 0.2 and 2 mL of PAA dissolved in 100 mL drinking water. Animals in Treatment Group 1 and 2 received 0.2% PAA daily for 4 weeks and 2% PAA daily for 4 weeks, respectively. After the animals had been sacrificed hematological parameters examined. Experimental results concerning this study were evaluated using SPSS v.11.5 and expressed as Mean SD p<0.05 was considered significant. Mean SD of WBC of groups 1 (2.45 0.77 and 2 (3.63 0.23 decreased significantly as compared with control group (5.3 0.57. RBC in control and 1, 2 groups were 8.34 0.39, 7.48 0.11 and 7.61 0.46, respectively. Also HCT and PLT decreased significantly in groups 1 and 2 as compared with control group. This study showed that oral consumption of Peracetic acid with concentration 0.2, 2% for 4 weeks can cause decrease hematological parameter in animal model.

  15. Early indications of soil recovery from acidic deposition in U.S. red spruce forests

    Science.gov (United States)

    Lawrence, Gregory B.; Shortle, Walter C.; David, Mark B.; Smith, Kevin T.; Warby, Richard A.F.; Lapenis, Andrei G.

    2012-01-01

    Forty to fifty percent decreases in acidic deposition through the 1980s and 1990s led to partial recovery of acidified surface waters in the northeastern United States; however, the limited number of studies that have assessed soil change found increased soil acidification during this period. From existing data, it's not clear whether soils continued to worsen in the 1990s or if recovery had begun. To evaluate possible changes in soils through the 1990s, soils in six red spruce (Picea rubens Sarg.) stands in New York, Vermont, New Hampshire, and Maine, first sampled in 1992 to 1993, were resampled in 2003 to 2004. The Oa-horizon pH increased (P 42−, which decreased the mobility of Al throughout the upper soil profile. Results indicate a nascent recovery driven largely by vegetation processes.

  16. Commercial double-indicator-dilution densitometer using heavy water: Evaluation in oleic-acid pulmonary edema

    Energy Technology Data Exchange (ETDEWEB)

    Leksell, L.G.; Schreiner, M.S.; Sylvestro, A.; Neufeld, G.R. (Univ. of Pennsylvania School of Medicine, Philadelphia (USA))

    1990-04-01

    We evaluated a commercially available, double-indicator-dilution densitometric system for the estimation of pulmonary extravascular water volume in oleic acid-induced pulmonary edema. Indocyanine green and heavy water were used as the nondiffusible and diffusible tracers, respectively. Pulmonary extravascular water volume, measured with this system, was 67% of the gravimetric value (r = 0.91), which was consistent with values obtained from the radioisotope methods. The measured volume was not influenced by changes in cardiac index over a range of 1 to 4 L.min.m2. This system is less invasive than the thermal-dye technique and has potential for repeated clinical measurements of pulmonary extravascular lung water and cardiac output.

  17. Synthesis and characterization of polyesters derived from glycerol and phthalic acid

    Directory of Open Access Journals (Sweden)

    Danilo Hansen Guimarães

    2007-09-01

    Full Text Available The production of polyester via polycondensation between glycerol and phthalic acid using dibutyltin dilaurate is reported. Three glycerol:phthalic acid molar ratio used for the bulk polymerization were: 2:2; 2:3 and 2:4. FTIR confirmed the esterification of glycerol by the acid for all the polymers. DSC indicated no crystallinity, although the XRD plots indicate a very incipient crystallinity for the polymers containing higher amounts of phthalic anhydride. Scanning electron microscopy results indicates high homogeneity for all the polymers prepared.

  18. Chlorophyll-derived fatty acids regulate expression of lipid metabolizing enzymes in liver - a nutritional opportunity

    Directory of Open Access Journals (Sweden)

    Wolfrum Christian

    2001-01-01

    Full Text Available Nutritional values of fatty acid classes are normally discussed on the basis of their saturated, monounsaturated and polyunsaturated structures with implicit understanding that they are straight-chain. Here we focus on chlorophyll-derived phytanic and pristanic acids that are minor isoprenoid branched-chain lipid constituents in food, but of unknown nutritional value. After describing the enzyme machinery that degrades these nutrient fatty acids in the peroxisome, we show by the criteria of a mouse model and of a human cell culture model that they induce with high potency expression of enzymes responsible for beta-oxidation of straight-chain fatty acids in the peroxisome. We summarize present mechanistic knowledge on fatty acid signaling to the nucleus, which involves protein/protein contacts between peroxisome proliferator activated receptor (PPAR and fatty acid binding protein (FABP. In this signaling event the branched-chain fatty acids are the most effective ones. Finally, on the basis of this nutrient-gene interaction we discuss nutritional opportunities and therapeutic aspects of the chlorophyll-derived fatty acids.

  19. Synthesis and preliminary evaluation of the antimicrobial activity of selected 3-benzofurancarboxylic acid derivatives.

    Science.gov (United States)

    Kossakowski, Jerzy; Krawiecka, Mariola; Kuran, Bozena; Stefańska, Joanna; Wolska, Irena

    2010-07-06

    Halogen derivatives of selected 3-benzofurancarboxylic acids were prepared using 6-acetyl-5-hydroxy-2-methyl-3-benzofuranocarboxylic acid as starting material. (1)H-NMR spectra were obtained for all of the synthesized structures, and for compound VI, an X-ray crystal structure was also obtained. All derivatives were tested for antimicrobial activity against a selection of Gram-positive cocci, Gram-negative rods and yeasts. Three compounds, III, IV, and VI, showed antimicrobial activity against Gram-positive bacteria (MIC 50 to 200 microg/mL). Compounds VI and III exhibited antifungal activity against the Candida strains C. albicans and C. parapsilosis (MIC-100 microg/mL).

  20. Novel self-associative and multiphase nanostructured soft carriers based on amphiphilic hyaluronic acid derivatives

    DEFF Research Database (Denmark)

    Eenschooten, Corinne; Vaccaro, Andrea; Delie, Florence

    2012-01-01

    The purpose of the present study was to investigate the physicochemical properties in aqueous media of amphiphilic hyaluronic acid (HA) derivatives obtained by reaction of HA’s hydroxyl groups with octenyl succinic anhydride (OSA). The self-associative properties of the resulting octenyl succinic...... anhydridemodified hyaluronic acid (OSA-HA) derivatives were studied by fluorescence spectroscopy using Nile Red as fluorophore. The morphology, size and surface charge of the OSA-HA assemblies were determined by transmission electron microscopy, dynamic light scattering and by measuring their electrophoretic...

  1. Synthesis, in vitro and in vivo antitumor activity of pyrazole-fused 23-hydroxybetulinic acid derivatives.

    Science.gov (United States)

    Zhang, Hengyuan; Zhu, Peiqing; Liu, Jie; Lin, Yan; Yao, Hequan; Jiang, Jieyun; Ye, Wencai; Wu, Xiaoming; Xu, Jinyi

    2015-02-01

    A collection of pyrazole-fused 23-hydroxybetulinic acid derivatives were designed, synthesized and evaluated for their antitumor activity. Most of the newly synthesized compounds exhibited significant antiproliferative activity. Especially compound 15e displayed the most potent activity with the IC50 values of 5.58 and 6.13μM against B16 and SF763 cancer cell lines, respectively. Furthermore, the significant in vivo antitumor activity of 15e was validated in H22 liver cancer and B16 melanoma xenograft mouse models. The structure-activity relationships of these 23-hydroxybetulinic acid derivatives were also discussed based on the present investigation.

  2. Promise of Retinoic Acid-Triazolyl Derivatives in Promoting Differentiation of Neuroblastoma Cells.

    Science.gov (United States)

    Lone, Ali Mohd; Dar, Nawab John; Hamid, Abid; Shah, Wajaht Amin; Ahmad, Muzamil; Bhat, Bilal A

    2016-01-20

    Retinoic acid induces differentiation in various types of cells including skeletal myoblasts and neuroblasts and maintains differentiation of epithelial cells. The present study demonstrates synthesis and screening of a library of retinoic acid-triazolyl derivatives for their differentiation potential on neuroblastoma cells. Click chemistry approach using copper(I)-catalyzed azide-alkyne cycloaddition was adopted for the preparation of these derivatives. The neurite outgrowth promoting potential of retinoic acid-triazolyl derivatives was studied on neuroblastoma cells. Morphological examination revealed that compounds 8a, 8e, 8f, and 8k, among the various derivatives screened, exhibited promising neurite-outgrowth inducing activity at a concentration of 10 μM compared to undifferentiated and retinoic acid treated cells. Further on, to confirm this differentiation potential of these compounds, neuroblastoma cells were probed for expression of neuronal markers such as NF-H and NeuN. The results revealed a marked increase in the NF-H and NeuN protein expression when treated with 8a, 8e, 8f, and 8k compared to undifferentiated and retinoic acid treated cells. Thus, these compounds could act as potential leads in inducing neuronal differentiation for future studies.

  3. Inhibitory effects of caffeic acid phenethyl ester derivatives on replication of hepatitis C virus.

    Directory of Open Access Journals (Sweden)

    Hui Shen

    Full Text Available Caffeic acid phenethyl ester (CAPE has been reported as a multifunctional compound. In this report, we tested the effect of CAPE and its derivatives on hepatitis C virus (HCV replication in order to develop an effective anti-HCV compound. CAPE and CAPE derivatives exhibited anti-HCV activity against an HCV replicon cell line of genotype 1b with EC50 values in a range from 1.0 to 109.6 µM. Analyses of chemical structure and antiviral activity suggested that the length of the n-alkyl side chain and catechol moiety are responsible for the anti-HCV activity of these compounds. Caffeic acid n-octyl ester exhibited the highest anti-HCV activity among the tested derivatives with an EC50 value of 1.0 µM and an SI value of 63.1 by using the replicon cell line derived from genotype 1b strain Con1. Treatment with caffeic acid n-octyl ester inhibited HCV replication of genotype 2a at a similar level to that of genotype 1b irrespectively of interferon signaling. Caffeic acid n-octyl ester could synergistically enhance the anti-HCV activities of interferon-alpha 2b, daclatasvir, and VX-222, but neither telaprevir nor danoprevir. These results suggest that caffeic acid n-octyl ester is a potential candidate for novel anti-HCV chemotherapy drugs.

  4. Technological and economic potential of poly(lactic acid) and lactic acid derivatives

    Energy Technology Data Exchange (ETDEWEB)

    Datta, R.; Tsai, S.P.; Bonsignore, P.; Moon, S.H.; Frank, J.R.

    1993-10-01

    Lactic acid has been an intermediate-volume specialty chemical (world production {approximately}40,000 tons/yr) used in a wide range of food processing and industrial applications. lactic acid h,as the potential of becoming a very large volume, commodity-chemical intermediate produced from renewable carbohydrates for use as feedstocks for biodegradable polymers, oxygenated chemicals, plant growth regulators, environmentally friendly ``green`` solvents, and specially chemical intermediates. In the past, efficient and economical technologies for the recovery and purification of lactic acid from crude fermentation broths and the conversion of tactic acid to the chemical or polymer intermediates had been the key technology impediments and main process cost centers. The development and deployment of novel separations technologies, such as electrodialysis (ED) with bipolar membranes, extractive distillations integrated with fermentation, and chemical conversion, can enable low-cost production with continuous processes in large-scale operations. The use of bipolar ED can virtually eliminate the salt or gypsum waste produced in the current lactic acid processes. In this paper, the recent technical advances in tactic and polylactic acid processes are discussed. The economic potential and manufacturing cost estimates of several products and process options are presented. The technical accomplishments at Argonne National Laboratory (ANL) and the future directions of this program at ANL are discussed.

  5. Paecilonic acids A and B, bicyclic fatty acids from the jellyfish-derived fungus Paecilomyces variotii J08NF-1.

    Science.gov (United States)

    Wang, Haibo; Hong, Jongki; Yin, Jun; Liu, Juan; Liu, Yonghong; Choi, Jae Sue; Jung, Jee H

    2016-05-01

    Two new bicyclic fatty acids, paecilonic acids A and B (1 and 2), were isolated from the culture broth of the marine fungus Paecilomyces variotii derived from the jellyfish Nemopilema nomurai. Compounds 1 and 2 share the same molecular formula and possess a 6,8-dioxabicyclo[3.2.1]octane core skeleton. The planar structures of compounds 1 and 2 were established by spectroscopic analysis, which included NMR and ESI-MS/MS. Relative and absolute configurations were determined by analyzing coupling constants, NOESY correlations, and optical rotations.

  6. Liver free fatty acid (FFA) accumulation as an indicator of ischemic injury during cold preservation

    Energy Technology Data Exchange (ETDEWEB)

    Nemoto, E.M.; Kang, Y.; DeWolf, A.M.; Lin, M.R.; Bleyaert, A.L.; Winter, P.M.

    1987-05-01

    Reliable assessment of hepatic viability prior to harvest and transplant could improve graft success and aid in evaluating the efficacy of liver preservation techniques. Hepatic tissue metabolites, protein (Pr) synthesis, and ATP have been studied, but none reliably correlate with hepatic viability. Therefore, they studied changes in liver FFA relative to changes in ATP and Pr synthesis during cold ischemic preservation. Rats mechanically ventilated on 0.5% isoflurane/70% N/sub 2/O/30% O/sub 2/ were heparinized and their livers perfused with air-equilibrated Euro-Collins solution (ECS) at 0-4/sup 0/C and kept on ice. A piece of the liver was removed after 0, 2, 6, 8, 12, 24, 36 and 48 h of preservation for ATP and FFA analysis. A portion of the liver was sliced (250 ..mu..m thick) and incubated in vitro for /sup 14/C-lysine incorporation in albumin. ATP, FFA and Pr synthesis were unchanged in the first 8 h, but markedly decreased between 8 and 12 h with little change thereafter. In contrast, between 8 and 48 h, arachidonic and stearic acids increased by 5 and 2-fold, respectively. Changes in ATP and Pr synthesis correlate with the empirically derived clinical maximum of 8 to 12 h preservation. FFA accumulation appears to reflect hepatic ischemic injury and may be a means of evaluating the quality of a donor liver.

  7. Derivation of multivariate indices of milk composition, coagulation properties, and individual cheese yield in dairy sheep.

    Science.gov (United States)

    Manca, M G; Serdino, J; Gaspa, G; Urgeghe, P; Ibba, I; Contu, M; Fresi, P; Macciotta, N P P

    2016-06-01

    Milk composition and its technological properties are traits of interest for the dairy sheep industry because almost all milk produced is processed into cheese. However, several variables define milk technological properties and a complex correlation pattern exists among them. In the present work, we measured milk composition, coagulation properties, and individual cheese yields in a sample of 991 Sarda breed ewes in 47 flocks. The work aimed to study the correlation pattern among measured variables and to obtain new synthetic indicators of milk composition and cheese-making properties. Multivariate factor analysis was carried out on individual measures of milk coagulation parameters; cheese yield; fat, protein, and lactose percentages; somatic cell score; casein percentage; NaCl content; pH; and freezing point. Four factors that were able to explain about 76% of the original variance were extracted. They were clearly interpretable: the first was associated with composition and cheese yield, the second with udder health status, the third with coagulation, and the fourth with curd characteristics. Factor scores were then analyzed by using a mixed linear model that included the fixed effect of parity, lambing month, and lactation stage, and the random effect of flock-test date. The patterns of factor scores along lactation stages were coherent with their technical meaning. A relevant effect of flock-test date was detected, especially on the 2 factors related to milk coagulation properties. Results of the present study suggest the existence of a simpler latent structure that regulates relationships between variables defining milk composition and coagulation properties in sheep. Heritability estimates for the 4 extracted factors were from low to moderate, suggesting potential use of these new variables as breeding goals.

  8. A Direct, Biomass-Based Synthesis of Benzoic Acid: Formic Acid-Mediated Deoxygenation of the Glucose-Derived Materials Quinic Acid and Shikimic Acid

    Energy Technology Data Exchange (ETDEWEB)

    Arceo, Elena; Ellman, Jonathan; Bergman, Robert

    2010-05-03

    An alternative biomass-based route to benzoic acid from the renewable starting materials quinic acid and shikimic acid is described. Benzoic acid is obtained selectively using a highly efficient, one-step formic acid-mediated deoxygenation method.

  9. Diversity in prokaryotic glycosylation: an archaeal-derived N-linked glycan contains legionaminic acid.

    Science.gov (United States)

    Kandiba, Lina; Aitio, Olli; Helin, Jari; Guan, Ziqiang; Permi, Perttu; Bamford, Dennis H; Eichler, Jerry; Roine, Elina

    2012-05-01

    VP4, the major structural protein of the haloarchaeal pleomorphic virus, HRPV-1, is glycosylated. To define the glycan structure attached to this protein, oligosaccharides released by β-elimination were analysed by mass spectrometry and nuclear magnetic resonance spectroscopy. Such analyses showed that the major VP4-derived glycan is a pentasaccharide comprising glucose, glucuronic acid, mannose, sulphated glucuronic acid and a terminal 5-N-formyl-legionaminic acid residue. This is the first observation of legionaminic acid, a sialic acid-like sugar, in an archaeal-derived glycan structure. The importance of this residue for viral infection was demonstrated upon incubation with N-acetylneuraminic acid, a similar monosaccharide. Such treatment reduced progeny virus production by half 4 h post infection. LC-ESI/MS analysis confirmed the presence of pentasaccharide precursors on two different VP4-derived peptides bearing the N-glycosylation signal, NTT. The same sites modified by the native host, Halorubrum sp. strain PV6, were also recognized by the Haloferax volcanii N-glycosylation apparatus, as determined by LC-ESI/MS of heterologously expressed VP4. Here, however, the N-linked pentasaccharide was the same as shown to decorate the S-layer glycoprotein in this species. Hence, N-glycosylation of the haloarchaeal viral protein, VP4, is host-specific. These results thus present additional examples of archaeal N-glycosylation diversity and show the ability of Archaea to modify heterologously expressed proteins.

  10. Associations of Milk Consumption and Vitamin B₂ and Β12 Derived from Milk with Fitness, Anthropometric and Biochemical Indices in Children. The Healthy Growth Study.

    Science.gov (United States)

    Moschonis, George; van den Heuvel, Ellen G H M; Mavrogianni, Christina; Singh-Povel, Cécile M; Leotsinidis, Michalis; Manios, Yannis

    2016-10-13

    The benefits of dairy consumption seem to extend beyond its significant contribution to ensuring nutrient intake adequacy as indicated by the favourable associations with several health outcomes reported by different studies. The aims of the present study were to examine the associations of milk consumption with fitness, anthropometric and biochemical indices in children and further explore whether the observed associations are attributed to vitamins B₂ and B12 derived from milk. A representative subsample of 600 children aged 9-13 years participating in the Healthy Growth Study was examined. Data were collected on children's dietary intake, using 24 h recalls, as well as on fitness, anthropometric and biochemical indices. Regression analyses were performed for investigating the research hypothesis, adjusting for potential confounders and for B-vitamin status indices (i.e., plasma riboflavin, methylmalonic acid and total homocysteine concentrations), dietary calcium intake and plasma zinc concentrations that could possibly act as effect modifiers. Milk consumption was positively associated with the number of stages performed in the endurance run test (ERT) (β = 0.10; p = 0.017) and negatively with body mass index (BMI) (β = -0.10; p = 0.014), after adjusting for several potential confounders and effect modifiers. Dietary intakes of vitamin B₂ and B12 derived from milk were also positively associated with the number of ERT stages (β = 0.10; p = 0.015 and β = 0.10; p = 0.014 respectively). In conclusion, higher intake of milk as well as vitamin B₂ and B12 derived from milk were independently associated with higher cardiorespiratory fitness in Greek preadolescents. The key roles of these B-vitamins in substrate oxidation, energy production, haemoglobin synthesis and erythropoiesis could provide a basis for interpreting these associations. However, further research is needed to confirm this potential interpretation.

  11. Study on reduction and back extraction of Pu(IV) by urea derivatives in nitric acid conditions

    Energy Technology Data Exchange (ETDEWEB)

    Ye, G.A.; Xiao, S.T.; Yan, T.H.; Lin, R.S.; Zhu, Z.W. [China Institute of Atomic Energy, P.O.Box 275(26), Beijing 102413 (China)

    2013-07-01

    The reduction kinetics of Pu(IV) by hydroxyl-semicarbazide (HSC), hydroxyurea (HU) and di-hydroxyurea (DHU) in nitric acid solutions were investigated separately with adequate kinetic equations. In addition, counter-current cascade experiments were conducted for Pu split from U in nitric acid media using three kinds of reductant, respectively. The results show that urea derivatives as a kind of novel salt-free reductant can reduce Pu(IV) to Pu(III) rapidly in the nitric acid solutions. The stripping experimental results showed that Pu(IV) in the organic phase can be stripped rapidly to the aqueous phase by the urea derivatives, and the separation factors of plutonium /uranium can reach more than 10{sup 4}. This indicates that urea derivatives is a kind of promising salt-free agent for uranium/plutonium separation. In addition, the complexing effect of HSC with Np(IV) was revealed, and Np(IV) can be back-extracted by HSC with a separation factor of about 20.

  12. Antihyperglycemic effects of gymnemic acid IV, a compound derived from Gymnema sylvestre leaves in streptozotocin-diabetic mice.

    Science.gov (United States)

    Sugihara, Y; Nojima, H; Matsuda, H; Murakami, T; Yoshikawa, M; Kimura, I

    2000-01-01

    We investigated the antihyperglycemic action of a crude saponin fraction and five triterpene glycosides (gymnemic acids I-IV and gymnemasaponin V) derived from the methanol extract of leaves of Gymnema sylvestre R. BR. (Asclepiadaceae) in streptozotocin (STZ)-diabetic mice. The saponin fraction (60mg/kg) reduced blood glucose levels 2 4h after the intraperitoneal administration. Gymnemic acid IV, not the other 4 glycosides at doses of 3.4-13.4mg/kg reduced the blood glucose levels by 13.5-60.0% 6h after the administration comparable to the potency of glibenclamide, and did not change the blood glucose levels of normal mice. Gymnemic acid IV at 13.4 mg/kg increased plasma insulin levels in STZ-diabetic mice. Gymnemic acid IV (1 mg/mL) did not inhibit alpha-glycosidase activity in the brush border membrane vesicles of normal rat small intestines. These results indicate that insulin-releasing action of gymnemic acid IV may contribute to the antihyperglycemic effect by the leaves of G. sylvestre. Gymnemic acid IV may be an anti-obese and antihyperglycemic pro-drug.

  13. Safety assessment of animal- and plant-derived amino acids as used in cosmetics.

    Science.gov (United States)

    Burnett, Christina; Heldreth, Bart; Bergfeld, Wilma F; Belsito, Donald V; Hill, Ronald A; Klaassen, Curtis D; Liebler, Daniel C; Marks, James G; Shank, Ronald C; Slaga, Thomas J; Snyder, Paul W; Andersen, F Alan

    2014-01-01

    The Cosmetic Ingredient Review Expert Panel (Panel) reviewed the safety of animal- and plant-derived amino acid mixtures, which function as skin and hair conditioning agents. The safety of α-amino acids as direct food additives has been well established, based on extensive research through acute and chronic dietary exposures and the Panel previously has reviewed the safety of individual α-amino acids in cosmetics. The Panel focused its review on dermal irritation and sensitization data relevant to the use of these ingredients in topical cosmetics. The Panel concluded that these 21 ingredients are safe in the present practices of use and concentration as used in cosmetics.

  14. Synthesis and quantitative structure-property relationships of side chain-modified hyodeoxycholic acid derivatives.

    Science.gov (United States)

    Sabbatini, Paola; Filipponi, Paolo; Sardella, Roccaldo; Natalini, Benedetto; Nuti, Roberto; Macchiarulo, Antonio; Pellicciari, Roberto; Gioiello, Antimo

    2013-08-30

    Bile acids have emerged as versatile signalling compounds of a complex network of nuclear and membrane receptors regulating various endocrine and paracrine functions. The elucidation of the interconnection between the biological pathways under the bile acid control and manifestations of hepatic and metabolic diseases have extended the scope of this class of steroids for in vivo investigations. In this framework, the design and synthesis of novel biliary derivatives able to modulate a specific receptor requires a deep understanding of both structure-activity and structure-property relationships of bile acids. In this paper, we report the preparation and the critical micellization concentration evaluation of a series of hyodeoxycholic acid derivatives characterized by a diverse side chain length and by the presence of a methyl group at the alpha position with respect to the terminal carboxylic acid moiety. The data collected are instrumental to extend on a quantitative basis, the knowledge of the current structure-property relationships of bile acids and will be fruitful, in combination with models of receptor activity, to design and prioritize the synthesis of novel pharmacokinetically suitable ligands useful in the validation of bile acid-responsive receptors as therapeutic targets.

  15. Synthesis and Quantitative Structure-Property Relationships of Side Chain-Modified Hyodeoxycholic Acid Derivatives

    Directory of Open Access Journals (Sweden)

    Antimo Gioiello

    2013-08-01

    Full Text Available Bile acids have emerged as versatile signalling compounds of a complex network of nuclear and membrane receptors regulating various endocrine and paracrine functions. The elucidation of the interconnection between the biological pathways under the bile acid control and manifestations of hepatic and metabolic diseases have extended the scope of this class of steroids for in vivo investigations. In this framework, the design and synthesis of novel biliary derivatives able to modulate a specific receptor requires a deep understanding of both structure-activity and structure-property relationships of bile acids. In this paper, we report the preparation and the critical micellization concentration evaluation of a series of hyodeoxycholic acid derivatives characterized by a diverse side chain length and by the presence of a methyl group at the alpha position with respect to the terminal carboxylic acid moiety. The data collected are instrumental to extend on a quantitative basis, the knowledge of the current structure-property relationships of bile acids and will be fruitful, in combination with models of receptor activity, to design and prioritize the synthesis of novel pharmacokinetically suitable ligands useful in the validation of bile acid-responsive receptors as therapeutic targets.

  16. Elevated antibody to D-alanyl lipoteichoic acid indicates caries experience associated with fluoride and gingival health

    OpenAIRE

    2002-01-01

    Background Acidogenic, acid-tolerant bacteria induce dental caries and require D-alanyl glycerol lipoteichoic acid (D-alanyl LTA) on their cell surface. Because fluoride inhibits acid-mediated enamel demineralization, an elevated antibody response to D-alanyl LTA may indicate subjects with more acidogenic bacteria and, therefore, an association of DMFT with fluoride exposure and gingival health not apparent in low responders. Methods Cluster analysis was used to identify low antibody content...

  17. Simultaneous determination of 2-naphthoxyacetic acid and indole-3-acetic acid by first derivation synchronous fluorescence spectroscopy.

    Science.gov (United States)

    Liu, Xiangxiang; Wan, Yiqun

    2013-07-01

    A simple, rapid, sensitive and selective method for simultaneously determining 2-naphthoxyacetic acid (BNOA) and Indole-3-Acetic Acid (IAA) in mixtures has been developed using derivation synchronous fluorescence spectroscopy based on their synchronous fluorescence. The synchronous fluorescence spectra were obtained with Δλ=100 nm in a pH 8.5 NaH2PO4-NaOH buffer solution, and the detected wavelengths of quantitative analysis were set at 239 nm for BNOA and 293 nm for IAA respectively. The over lapped fluorescence spectra were well separated by the synchronous derivative method. Under optimized conditions, the limits of detection (LOD) were 0.003 μg/mL for BNOA and 0.012 μg/mL for IAA. This method is simple and expeditious, and it has been successfully applied to the determination of 2-naphthoxyacetic acid and indole-3-acetic acid in fruit juice samples with satisfactory results. The samples were only filtrated through a 0.45 μm membrane filter, which was free from the tedious separation procedures. The obtaining recoveries were in the range of 83.88-87.43% for BNOA and 80.76-86.68% for IAA, and the relative standard deviations were all less than 5.0%. Statistical comparison of the results with high performance liquid chromatography Mass Spectrometry (HPLC-MS) method revealed good agreement and proved that there were no significant difference in the accuracy and precision between these two methods.

  18. Simultaneous determination of 2-naphthoxyacetic acid and indole-3-acetic acid by first derivation synchronous fluorescence spectroscopy

    Science.gov (United States)

    Liu, Xiangxiang; Wan, Yiqun

    2013-07-01

    A simple, rapid, sensitive and selective method for simultaneously determining 2-naphthoxyacetic acid (BNOA) and Indole-3-Acetic Acid (IAA) in mixtures has been developed using derivation synchronous fluorescence spectroscopy based on their synchronous fluorescence. The synchronous fluorescence spectra were obtained with Δλ = 100 nm in a pH 8.5 NaH2PO4-NaOH buffer solution, and the detected wavelengths of quantitative analysis were set at 239 nm for BNOA and 293 nm for IAA respectively. The over lapped fluorescence spectra were well separated by the synchronous derivative method. Under optimized conditions, the limits of detection (LOD) were 0.003 μg/mL for BNOA and 0.012 μg/mL for IAA. This method is simple and expeditious, and it has been successfully applied to the determination of 2-naphthoxyacetic acid and indole-3-acetic acid in fruit juice samples with satisfactory results. The samples were only filtrated through a 0.45 μm membrane filter, which was free from the tedious separation procedures. The obtaining recoveries were in the range of 83.88-87.43% for BNOA and 80.76-86.68% for IAA, and the relative standard deviations were all less than 5.0%. Statistical comparison of the results with high performance liquid chromatography Mass Spectrometry (HPLC-MS) method revealed good agreement and proved that there were no significant difference in the accuracy and precision between these two methods.

  19. Growth behavior of anodic oxide formed by aluminum anodizing in glutaric and its derivative acid electrolytes

    Science.gov (United States)

    Nakajima, Daiki; Kikuchi, Tatsuya; Natsui, Shungo; Suzuki, Ryosuke O.

    2014-12-01

    The growth behavior of anodic oxide films formed via anodizing in glutaric and its derivative acid solutions was investigated based on the acid dissociation constants of electrolytes. High-purity aluminum foils were anodized in glutaric, ketoglutaric, and acetonedicarboxylic acid solutions under various electrochemical conditions. A thin barrier anodic oxide film grew uniformly on the aluminum substrate by glutaric acid anodizing, and further anodizing caused the film to breakdown due to a high electric field. In contrast, an anodic porous alumina film with a submicrometer-scale cell diameter was successfully formed by ketoglutaric acid anodizing at 293 K. However, the increase and decrease in the temperature of the ketoglutaric acid resulted in non-uniform oxide growth and localized pitting corrosion of the aluminum substrate. An anodic porous alumina film could also be fabricated by acetonedicarboxylic acid anodizing due to the relatively low dissociation constants associated with the acid. Acid dissociation constants are an important factor for the fabrication of anodic porous alumina films.

  20. Multilayer Film Fabrication and Photoelectric Conversion Property of Two Pyrrolidinofullerene Carboxylic Acid Derivatives

    Institute of Scientific and Technical Information of China (English)

    2000-01-01

    Two multilayer films of pyrrolidinofullerene carboxylic acid derivatives, which exhibit photoelectric conversion property, are reported here. The first monolayers were fabricated on hydrophilic indium-tin-oxide (ITO), quartz, and mica by esterification reaction. The multilayers were characterized by contact angle and UV spectrum. The photoelectric conversion properties of both multilayer films were studied.

  1. Heterogeneous catalysts for the transformation of fatty acid triglycerides and their derivatives to fuel hydrocarbons

    Science.gov (United States)

    Yakovlev, Vadim A.; Khromova, Sofia A.; Bukhtiyarov, Valerii I.

    2011-10-01

    The results of studies devoted to the catalysts for transformation of fatty acid triglycerides and their derivatives to fuel hydrocarbons are presented and described systematically. Various approaches to the use of heterogeneous catalysts for the production of biofuel from these raw materials are considered. The bibliography includes 134 references.

  2. Syntheses of Nucleoside Derivatives Containing Fmoc- or Trityl-protected Amino Acids

    Institute of Scientific and Technical Information of China (English)

    GUO Hui; ZOU Wu-xin; JI Qi; MA Yu-xin; MENG Ji-ben

    2005-01-01

    Facile direct esterification reactions between 2′,3′-O-isopropylidene-nucleosides and Fmoc- or trityl-protected amino acids via N,N-dicyclohexyl-carbodiimide(DCC) mediated condensation are described. These reactions offer a mild and convenient method to synthesize aminoacylated nucleoside derivatives.

  3. Nonmetal catalyzed insertion reactions of diazocarbonyls to acid derivatives in fluorinated alcohols.

    Science.gov (United States)

    Dumitrescu, Lidia; Azzouzi-Zriba, Kaouther; Bonnet-Delpon, Danièle; Crousse, Benoit

    2011-02-18

    The insertion reaction of diazocarbonyls to acids could be performed smoothly in fluorinated alcohols in the absence of metal catalyst. This new procedure allowed the chemoselective preparation of various functionalized compounds such as acyloxyesters, depsipeptides, and sulfonate, phosphonate, or boronate derivatives.

  4. Aggregation behavior of cholic acid derivatives in organic solvents and in water

    NARCIS (Netherlands)

    Willemen, H.M.

    2002-01-01

    In this thesis various cholic acid derivatives are reported that display aggregation in water or in organic solvents. Spontaneous aggregation of single molecules into larger, ordered structures occurs at the borderline of solubility. Amphiphilic compounds, or surfactants, which possess a hydrophobic

  5. Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 1

    DEFF Research Database (Denmark)

    Rist, Oystein; Grimstrup, Marie; Receveur, Jean-Marie;

    2009-01-01

    Structure-activity relationships of three related series of 4-phenylthiazol-5-ylacetic acids, derived from two hits emanating from a focused library obtained by in silico screening, have been explored as CRTH2 (chemoattractant receptor-homologous molecule expressed on Th2 cells) antagonists. Seve...

  6. Antioxidant glucosylated caffeoylquinic acid derivatives in the invasive tropical soda apple, Solanum viarum

    Science.gov (United States)

    The eggplant (Solanum melongena) and other species within the “spiny solanums” (Solanum subgenus Leptostemonum) contain diverse and abundant antioxidant caffeoylquinic acid (CQA) derivatives. The fruit of an aggressive invasive species in the spiny solanums, Solanum viarum, contain numerous CQA deri...

  7. Synthesis and bioactivity of novel nitric oxide-releasing ursolic acid derivatives

    Institute of Scientific and Technical Information of China (English)

    Li Chen; Wen Qiu; Jia Tang; Zhi Feng Wang; Shu Ying He

    2011-01-01

    A series of furoxan-based novel nitric oxide-donating ursolic acid (UA) derivatives (7a-f) were synthesized, and their cytotoxic activities against HepG2 cells in vitro were evaluated by MTT method. It was found that 7a-d and 7f showed more potent cytotoxic activities than control 5-fluorouracil and UA.

  8. Parallel synthesis of arrays of amino-acid-derived isocyanoamides useful as starting materials in IMCR

    NARCIS (Netherlands)

    Dömling, Alexander; Beck, Barbara; Fuchs, Thilo; Yazbak, Ahmad

    2006-01-01

    Arrays of amino-acid-derived isocyanoamides are conveniently produced on a multigram scale in one step by the solventless aminolysis of the corresponding methyl esters with primary or secondary aliphatic amines. Most of the corresponding isocyanides precipitate during the reaction and can be filtere

  9. Synthesis of Boswellic Acid Derivatives and Primary Research on their Activities

    Institute of Scientific and Technical Information of China (English)

    Yan Qiu MENG; Lin Xiang ZHAO; Zan WANG; Dan LIU; Yong Kui JING

    2005-01-01

    In order to search for new potent anti-cancer agents, a series of boswellic acid derivatives were designed and synthesized. Six of them were identified by IR, NMR and MS as new compounds and biologic assay of anti-cancer is underway.

  10. Asymmetric and efficient synthesis of homophenylalanine derivatives via Friedel-Crafts reaction with trifluoromethanesulfonic acid

    OpenAIRE

    Murashige, Ryo; Hayashi, Yuka; Hashimoto, Makoto; 橋本, 誠

    2008-01-01

    An efficient Friedel-Crafts reaction of TFA-Asp(Cl)-OMe and stoichiometric amounts of benzene was established by using neat trifluoromethanesulfonic acid (TfOH) as solvent and catalyst under a mild condition. This methodology has been applied to many aromatic compounds and enabled synthesis of several homophenylalanine derivatives.

  11. An Unexpected and Efficient Synthesis of Open-chain Derivatives of Bistetronic Acid under Microwave Irradiation

    Institute of Scientific and Technical Information of China (English)

    SHI Feng; MA Ning; ZHOU Dianxiang; ZHANG Ge; JIANG Bo; TU Shujiang

    2009-01-01

    An unexpected and efficient synthesis of novel open-chain derivatives of bistetronic acid has been successfully achieved in glyclol under microwave irradiation (MW).This method has the prominent advantages of short reaction time,high yield,operational simplicity as well as environmental friendliness.

  12. Studies on chemical modification and biology of a natural product, gambogic acid (II): Synthesis and bioevaluation of gambogellic acid and its derivatives from gambogic acid as antitumor agents.

    Science.gov (United States)

    Wang, Jinxin; Ma, Junhai; You, Qidong; Zhao, Li; Wang, Fan; Li, Chong; Guo, Qinglong

    2010-09-01

    Gambogic acid (GA) has been reported to be a potent apoptosis inducer. The fact that it is amenable to chemical modification makes GA an attractive molecule for the development of anticancer agents. We firstly reported the synthesis of gambogellic acid, which was generated under acid catalysis from readily available GA by a base-catalyzed diene intramolecular annelation. Sequentially, thirteen new compounds were synthesized and their inhibitory activity on HT-29, Bel-7402, BGC-823, and A549 cell lines were evaluated in vitro by MTT assay, and (38, 40)-epoxy-33-chlorogambogellic acid (4) was identified as a BGC-823 cell apoptosis inducer through MTT cell assay, observations of morphological changes, and Annexin-V/PI double-staining assay. Compound 4 showed significant effects in inducing apoptosis and might serve as a potential lead compound for discovery of new anticancer drugs. Further structure-activity relationships (SARs) of gambogic acid derivatives were discussed.

  13. Evaluation of preservative effectiveness of p-coumaric acid derivatives in aluminium hydroxide gel-USP

    Directory of Open Access Journals (Sweden)

    Anurag Khatkar

    2013-01-01

    Full Text Available Background: Deterioration of pharmaceutical preparations due to growth of microorganisms is a great challenge and need of preservation becomes very important. Literature reports about various problems associated with the existing synthetic preservatives such as development of microbial resistance (in due course of time and several serious side effects. Aim: The aim of the present study is to find out new preservatives synthesized from natural sources, which may have better efficiency than the existing synthetic preservatives. The derivatives of naturally occurring p-coumaric acid were subjected for their preservative efficacy study. Their preservative efficiency was evaluated and compared with the standard parabens. Materials and Methods: The selected amide, anilide and ester derivatives of p-coumaric acid were subjected to preservative efficacy testing in an official antacid preparation, (aluminium hydroxide gel-USP against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Candida albicans and Aspergillus niger as representative challenging microorganisms as per USP 2004 guidelines. Results: The selected derivatives were found to be effective against all selected strains and showed preservative efficacy comparable to that of standard and even better in case E. coli, C. albicans and A. niger. The 8-hydroxy quinoline ester derivative showed better preservative efficacy than standard as well as other derivatives. Conclusion: The newly synthesized p- coumaric acid preservatives were found to be effective in the proposed pharmaceutical preparation (Aluminium Hydroxide Gel - USP. Also, the synthesized preservatives have shown comparative and even better efficacy than the existing parabens and hence they have potential for use in pharmaceutical preparations.

  14. Evaluation of preservative effectiveness of gallic acid derivatives in aluminum hydroxide gel-USP

    Directory of Open Access Journals (Sweden)

    Anurag Khatkar

    2013-01-01

    Full Text Available Background: Preservatives are added to most of the pharmaceutical preparations to prevent them from deterioration throughout their shelf life. Literature reveals that the common synthetic preservatives have many limitations, such as development of microbial resistance (in due course of time and several serious side-effects. Aim: The aim of this study is to find out new preservatives synthesized from natural sources, which may have better efficiency than the existing synthetic preservatives. The derivatives of naturally occurring gallic acid were subjected for their preservative efficacy study. Their preservative efficiency was evaluated and compared with the standard parabens. Materials and Methods: The selected amide, anilide and ester derivatives of gallic acid were subjected to preservative efficacy testing in an official antacid preparation, {aluminum hydroxide gel-USP (United States Pharmacopoeia} against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Candida albicans, and Aspergillus niger as representative challenging microorganisms as per USP 2004 guidelines. Results: The selected derivatives were found to be effective against all selected strains and showed preservative efficacy comparable to that of standard and even better in case E. coli, C. albicans and A. niger. The 8-hydroxy quinoline ester derivative showed better preservative efficacy than standard as well as other derivatives. Conclusion: The newly synthesized gallic acid preservatives were found to be effective in the proposed pharmaceutical preparation (Aluminium Hydroxide Gel - USP. Also, the synthesized preservatives have shown comparative and even better efficacy than the existing parabens and hence they have potential for use in pharmaceutical preparations.

  15. Investigations of the inhibition of copper corrosion in nitric acid solutions by ketene dithioacetal derivatives

    Energy Technology Data Exchange (ETDEWEB)

    Fiala, A. [Laboratoire de chimie moleculaire du controle de l' environnement et des mesures physico-chimiques, faculte des sciences exactes, universite Mentouri-Constantine, route de Ain-El-Bey, Constantine (Algeria)], E-mail: abdelfiala@yahoo.fr; Chibani, A. [Laboratoire de chimie moleculaire du controle de l' environnement et des mesures physico-chimiques, faculte des sciences exactes, universite Mentouri-Constantine, route de Ain-El-Bey, Constantine (Algeria); Darchen, A. [Laboratoire d' electrochimie, ecole nationale superieure de chimie de Rennes, avenue du general-Leclerc, 35700 Rennes (France); Boulkamh, A.; Djebbar, K. [Laboratoire de chimie moleculaire du controle de l' environnement et des mesures physico-chimiques, faculte des sciences exactes, universite Mentouri-Constantine, route de Ain-El-Bey, Constantine (Algeria)

    2007-10-15

    Ketene dithioacetal derivatives, namely 3-[bis(methylthio)methylene] pentane-2,4-dione (1), 3-(1,3-dithian-2-ylidene) pentane-2,4-dione (2) and 3-(1,3-dithiolan-2-ylidene) pentane-2,4-dione (3) were synthesized and their respective capacity to inhibit copper corrosion in 3 M HNO{sub 3} was investigated by means of weight loss, potentiodynamic polarization, scanning electron microscopy (SEM) and energy dispersive X-ray fluorescence (XRF). The obtained results indicate that the addition of these compounds significantly decreases the corrosion rate. Potentiodynamic polarization studies clearly showed that the inhibition efficiency increases with increasing concentration of the investigated compounds at a fixed temperature, but decreases with increasing temperature. These results on the whole showed that the studied substances are good cathodic inhibitors for copper corrosion in nitric acid medium. SEM and energy dispersive X-ray (EDAX) examination of the copper surface revealed that these compounds prevented copper from corrosion by adsorption on its surface to form a protective film, which acts as a barrier to aggressive agents. The presence of these organic compounds adsorbed on the electrode surface was confirmed by XRF investigations.

  16. Synthesis and Characterization of Nanosized Uranyl Coordination Polymers derived from Terephthalic acid and Azoles

    Directory of Open Access Journals (Sweden)

    Maged S.Al-Fakeh

    2016-05-01

    Full Text Available The structure of the complexes [UO2(TPA(Azole(H2O].xH2O, TPA = 1,4-benzenedicarboxylic acid and azoles = 2-aminobenzothiazole, 2-aminothiazole, 2-amino-4-methylthiazole and 2-mercaptobenzothiazole has been prepared and characterized. The structure of the complexes has been assigned based on elemental analysis, IR, electronic spectral studies, magnetic measurement, molar conductance, Scanning electron microscope (S.E.M, X-ray powder diffraction techniques investigations and thermogravimetric analysis complete the characterization of the compound. Thermogravimetry(TG, derivative thermogravimetry (DTG and differential thermal analysis (DTA have been used to study the thermal decomposition of the complexes. The kinetic parameters have been calculated making use of the Coats-Redfern and Horowitz-Metzger. The scanning electron microscope SEM photographs and particle size calculations from the powder XRD data indicate the average size of the prepared UO2(II (28-56 nm supramolecular coordination polymers in the nanoscale range. The biological screening of the compounds was also tested.

  17. Medicinal importance of gallic acid and its ester derivatives: a patent review.

    Science.gov (United States)

    Choubey, Sneha; Varughese, Lesley Rachel; Kumar, Vinod; Beniwal, Vikas

    2015-01-01

    Gallic acid and its derivatives have a large number of applications in various fields of science. In nature, these compounds are widely distributed in plants and fruits, and thus they are being used as food stuffs, preservatives, etc. directly or indirectly by human community. They have also been implicated as anticarcinogenic, antimicrobial, antimutagenic, antiangiogenic and anti-inflammatory agents besides their use in treating critical diseases like depression, cancer, microbial infections, lipid-related diseases, etc. Herein, an attempt has been made to summarize the important uses of gallic acid derivatives which have extensively been disclosed particularly in various patents. This review would certainly create a great interest of the scientific community toward the developments and uses of gallic acid based compounds in the future.

  18. Spectroscopic studies on gallic acid and its azo derivatives and their iron(III) complexes.

    Science.gov (United States)

    Masoud, Mamdouh S; Ali, Alaa E; Haggag, Sawsan S; Nasr, Nessma M

    2014-01-01

    Azo gallic derivatives and their iron(III) complexes were synthesized and characterized. The stereochemistry and the mode of bonding of the complexes were achieved based on elemental analysis, UV-Vis and IR. The thermal behaviors of the complexes were studied. The effect of pH on the electronic absorption spectra of gallic acid and its azo derivatives are discussed. Different spectroscopic methods (molar ratio, straight line method, continuous variation, slope ratio and successive method) are applied for determination of stoichiometry and pK values for the complex formation of gallic acid with iron(III) in aqueous media. Iron(III) complexes of gallic acid is formed with different ratio: 1:1, 1:2, 1:3 and 1:4 (M:L).

  19. Semi-Empirical Predictions on the Structure and Properties of ent-Kaurenoic Acid and Derivatives

    Directory of Open Access Journals (Sweden)

    Jose Isagani B. Janairo

    2011-01-01

    Full Text Available The physicochemical properties of ent- kaurenoic acid model derivatives, which possibly influence its therapeutic application, were calculated. Results revealed that the molecule possess favourable attributes which renders it possible to be considered as a drug lead only that its very hydrophobic nature can result to poor bioavailabilty, low absorption and poor systemic circulation. In silico simulations revealed that this setback can be overcome by introduction of hydroxyl group to the tertiary carbon of ent-kaurenoic acid employing m-CPBA catalyzed hydroxylation, thus, unleashing its full drug potency. Moreover, molecular similarity analyses derived from semi-empirical calculations between ent-kaurenoic acid and a set of kaurane diterpenoids showed differences in hydrophobic complementarity, size and electronic properties despite possessing nearly identical molecular frameworks, thus, arriving in a generalization for their observed mechanistic differences on acting on different targets.

  20. Production of fatty acid-derived oleochemicals and biofuels by synthetic yeast cell factories

    DEFF Research Database (Denmark)

    Zhou, Yongjin J.; Buijs, Nicolaas A; Zhu, Zhiwei

    2016-01-01

    -level production of free fatty acids (FFAs) in a yeast cell factory, and the production of alkanes and fatty alcohols from its descendants. The engineered strain produces up to 10.4 g l−1 of FFAs, which is the highest reported titre to date. Furthermore, through screening of specific pathway enzymes, endogenous...... alcohol dehydrogenases and aldehyde reductases, we reconstruct efficient pathways for conversion of fatty acids to alkanes (0.8 mg l−1) and fatty alcohols (1.5 g l−1), to our knowledge the highest titres reported in S. cerevisiae. This should facilitate the construction of yeast cell factories...... for production of fatty acids derived products and even aldehyde-derived chemicals of high value....

  1. Synthesis, saccharide-binding and anti-cancer cell proliferation properties of arylboronic acid derivatives of indoquinolines.

    Science.gov (United States)

    Meng, Junxiu; Yu, Shaoqing; Wan, Shengbiao; Ren, Sumei; Jiang, Tao

    2011-11-01

    A facile synthesis of a series of saccharide-binding arylboronic acid derivatives of indoloquinoline was described. The key synthetic steps were polyphosphoric acid-mediated cyclization, chlorinative aromatization, and amidation. Mass spectrometry experiments revealed these synthetic arylboronic acid derivatives of indoquinolines could bind to biologically important carbohydrates (sialic acid, fucose, glucose, and galactose) by forming boronate di-esters in alkaline aqueous solution. Most of the arylboronic acid derivatives of indoquinolines inhibited human breast cancer cell (MDA-231) proliferation at a concentration of 5 μm, whereas the compound 17 exhibited highest percentages (76.74%) of the cancer cell proliferation inhibition.

  2. Synthesis, structure and cytotoxic activity of acetylenic derivatives of betulonic and betulinic acids

    Science.gov (United States)

    Bębenek, Ewa; Chrobak, Elwira; Wietrzyk, Joanna; Kadela, Monika; Chrobak, Artur; Kusz, Joachim; Książek, Maria; Jastrzębska, Maria; Boryczka, Stanisław

    2016-02-01

    A series of acetylenic derivatives of betulonic and betulinic acids has been synthesized and characterized by 1H and 13C NMR, IR and MS spectroscopy. The structure of propargyl betulonate 4 and propargyl betulinate-DMF solvate 8A was solved by X-ray diffraction. Thermal properties were examined using a DSC technique. The resulting alkynyl derivatives, as well as betulin 1 and betulinic acid 3, were evaluated in vitro for their cytotoxic activity against human T47D breast cancer, CCRF/CEM leukemia, SW707 colorectal, murine P388 leukemia and BALB3T3 normal fibroblasts cell lines. Several of the obtained compounds have a favorable cytotoxic profile than betulin 1. Propargyl betulinate 8 was the most active derivative, being up to 3-fold more potent than betulin 1 against the human leukemia (CCRF/CEM) cell line, with an IC50 value of 3.9 μg/mL.

  3. In situ forming hydrogels of hyaluronic acid and inulin derivatives for cartilage regeneration.

    Science.gov (United States)

    Palumbo, Fabio S; Fiorica, Calogero; Di Stefano, Mauro; Pitarresi, Giovanna; Gulino, Alessandro; Agnello, Stefano; Giammona, Gaetano

    2015-05-20

    An in situ forming hydrogel obtained by crosslinking of amino functionalized hyaluronic acid derivatives with divinylsulfone functionalized inulin (INU-DV) has been here designed and characterized. In particular two hyaluronic acid derivatives bearing respectively a pendant ethylenediamino (EDA) portion (HA-EDA) and both EDA and octadecyl pendant groups (HA-EDA-C18) were crosslinked through an azo-Michael reaction with INU-DV. Gelation time and consumption of DV portions have been evaluated on hydrogel obtained using HA-EDA and HA-EDA-C18 derivatives with a concentration of 3% w/v and a ratio 80/20 w/w respect to the crosslinker INU-DV. The presence of pendant C18 chains improves mechanical performances of hydrogels and decreases the susceptibility to hyaluronidase hydrolysis. Bovine chondrocytes, encapsulated during crosslinking, sufficiently survive and efficiently proliferate until 28 days of analysis.

  4. TEMPORAL AND SPATIAL ANALYSES OF SPECTRAL INDICES OF NONTHERMAL EMISSIONS DERIVED FROM HARD X-RAYS AND MICROWAVES

    Energy Technology Data Exchange (ETDEWEB)

    Asai, Ayumi [Unit of Synergetic Studies for Space, Kyoto University, Yamashina, Kyoto, 607-8471 (Japan); Kiyohara, Junko; Takasaki, Hiroyuki [Kwasan and Hida Observatories, Kyoto University, Yamashina, Kyoto, 607-8471 (Japan); Narukage, Noriyuki [Institute of Space and Astronomical Science, Japan Aerospace Exploration Agency, Chuo, Sagamihara, Kanagawa, 229-8510 (Japan); Yokoyama, Takaaki [Department of Earth and Planetary Science, University of Tokyo, Hongo, Bunkyo, Tokyo, 113-0033 (Japan); Masuda, Satoshi [Solar-Terrestrial Environment Laboratory, Nagoya University, Chikusa, Nagoya, Aichi, 464-8601 (Japan); Shimojo, Masumi [National Astronomical Observatory of Japan, Mitaka, Tokyo, 181-8588 (Japan); Nakajima, Hiroshi, E-mail: asai@kwasan.kyoto-u.ac.jp [Nobeyama Solar Radio Observatory, National Astronomical Observatory of Japan, Minamimaki, Minamisaku, Nagano, 384-1305 (Japan)

    2013-02-15

    We studied electron spectral indices of nonthermal emissions seen in hard X-rays (HXRs) and microwaves. We analyzed 12 flares observed by the Hard X-Ray Telescope aboard Yohkoh, Nobeyama Radio Polarimeters, and the Nobeyama Radioheliograph (NoRH), and compared the spectral indices derived from total fluxes of HXRs and microwaves. Except for four events, which have very soft HXR spectra suffering from the thermal component, these flares show a gap {Delta}{delta} between the electron spectral indices derived from HXRs {delta} {sub X} and those from microwaves {delta}{sub {mu}} ({Delta}{delta} = {delta} {sub X} - {delta}{sub {mu}}) of about 1.6. Furthermore, from the start to the peak times of the HXR bursts, the time profiles of the HXR spectral index {delta} {sub X} evolve synchronously with those of the microwave spectral index {delta}{sub {mu}}, keeping the constant gap. We also examined the spatially resolved distribution of the microwave spectral index by using NoRH data. The microwave spectral index {delta}{sub {mu}} tends to be larger, which means a softer spectrum, at HXR footpoint sources with stronger magnetic field than that at the loop tops. These results suggest that the electron spectra are bent at around several hundreds of keV, and become harder at the higher energy range that contributes the microwave gyrosynchrotron emission.

  5. The effect of water, ascorbic acid, and cranberry derived supplementation on human urine and uropathogen adhesion to silicone rubber

    NARCIS (Netherlands)

    Habash, MB; Van der Mei, HC; Busscher, HJ; Reid, G

    1999-01-01

    In this study, urine was collected from groups of volunteers following the consumption of water, ascorbic acid, or cranberry supplements. Only ascorbic acid intake consistently produced acidic urine. Photospectroscopy data indicated that increased water consumption produced urine with lower protein

  6. Multicomponent click synthesis of new 1,2,3-triazole derivatives of pyrimidine nucleobases: promising acidic corrosion inhibitors for steel.

    Science.gov (United States)

    González-Olvera, Rodrigo; Espinoza-Vázquez, Araceli; Negrón-Silva, Guillermo E; Palomar-Pardavé, Manuel E; Romero-Romo, Mario A; Santillan, Rosa

    2013-12-06

    A series of new mono-1,2,3-triazole derivatives of pyrimidine nucleobases were synthesized by one-pot copper(I)-catalyzed 1,3-dipolar cycloaddition reactions between N-1-propargyluracil and thymine, sodium azide and several benzyl halides. The desired heterocyclic compounds were obtained in good yields and characterized by NMR, IR, and high resolution mass spectrometry. These compounds were investigated as corrosion inhibitors for steel in 1 M HCl solution, using electrochemical impedance spectroscopy (EIS) technique. The results indicate that these heterocyclic compounds are promising acidic corrosion inhibitors for steel.

  7. Selective binding of glutathione conjugates of fatty acid derivatives by plant glutathione transferases.

    Science.gov (United States)

    Dixon, David P; Edwards, Robert

    2009-08-07

    Proteomic studies with Arabidopsis thaliana have revealed that the plant-specific Tau (U) class glutathione transferases (GSTs) are selectively retained by S-hexylglutathione affinity supports. Overexpression of members of the Arabidopsis GST superfamily in Escherichia coli showed that 25 of the complement of 28 GSTUs caused the aberrant accumulation of acylated glutathione thioesters in vivo, a perturbation that was not observed with other GST classes. Each GSTU caused a specific group of fatty acyl derivatives to accumulate, which varied in chain length (C(6) to C(18)), additional oxygen content (0 or 1), and desaturation (0 or 1). Thioesters bound tightly to recombinant GSTs (K(d) approximately 1 microm), explaining their accumulation. Transient expression of GSTUs in Nicotiana benthamiana followed by recovery by Strep-tag affinity chromatography allowed the respective plant ligands to be extracted and characterized. Again, each GST showed a distinct profile of recovered metabolites, notably glutathionylated oxophytodienoic acid and related oxygenated fatty acids. Similarly, the expression of the major Tau protein GSTU19 in the endogenous host Arabidopsis led to the selective binding of the glutathionylated oxophytodienoic acid-glutathione conjugate, with the enzyme able to catalyze the conjugation reaction. Additional ligands identified in planta included other fatty acid derivatives including divinyl ethers and glutathionylated chlorogenic acid. The strong and specific retention of various oxygenated fatty acids by each GSTU and the conservation in binding observed in the different hosts suggest that these proteins have selective roles in binding and conjugating these unstable metabolites in vivo.

  8. Potential Biological Applications of Bio-Based Anacardic Acids and Their Derivatives

    Directory of Open Access Journals (Sweden)

    Fatma B. Hamad

    2015-04-01

    Full Text Available Cashew nut shells (CNS, which are agro wastes from cashew nut processing factories, have proven to be among the most versatile bio-based renewable materials in the search for functional materials and chemicals from renewable resources. CNS are produced in the cashew nut processing process as waste, but they contain cashew nut shell liquid (CNSL up to about 30–35 wt. % of the nut shell weight depending on the method of extraction. CNSL is a mixture of anacardic acid, cardanol, cardol, and methyl cardol, and the structures of these phenols offer opportunities for the development of diverse products. For anacardic acid, the combination of phenolic, carboxylic, and a 15-carbon alkyl side chain functional group makes it attractive in biological applications or as a synthon for the synthesis of a multitude of bioactive compounds. Anacardic acid, which is about 65% of a CNSL mixture, can be extracted from the agro waste. This shows that CNS waste can be used to extract useful chemicals and thus provide alternative green sources of chemicals, apart from relying only on the otherwise declining petroleum based sources. This paper reviews the potential of anacardic acids and their semi-synthetic derivatives for antibacterial, antitumor, and antioxidant activities. The review focuses on natural anacardic acids from CNS and other plants and their semi-synthetic derivatives as possible lead compounds in medicine. In addition, the use of anacardic acid as a starting material for the synthesis of various biologically active compounds and complexes is reported.

  9. Synthesis of benzamide derivatives of anacardic acid and their cytotoxic activity.

    Science.gov (United States)

    Chandregowda, Venkateshappa; Kush, Anil; Reddy, Goukanapalli Chandrasekara

    2009-06-01

    Several benzamide derivatives were synthesized from anacardic acid (1a) which was the product of hydrogenation of the naturally occurring anacardic acid mixture (1a-d), a major constituent of cashew nut shell liquid. Anacardic acid (1a) was first alkylated followed by hydrolysis of the ester to obtain synthones namely, 2-ethoxy-6-pentadecylbenzoic acid (5) and 2-isopropoxy-6-pentadecylbenzoic acid (6). These salicylic acid derivatives were then coupled with a variety of anilines to obtain novel benzamide compounds (7-39). Cytotoxic effect of these synthesized compounds was tested on HeLa cell line of wild type with relatively high expression of p300 and on HCT-15, which is p300 negative. Of all the compounds, 2-isopropoxy-6-pentadecyl-N-pyridin-4-ylbenzamide (27), 2-ethoxy-N-(3-nitrophenyl)-6-pentadecylbenzamide (22) and 2-ethoxy-6-pentadecyl-N-pyridin-4-ylbenzamide (10) were found to be more potent with the respective IC(50) values 11.02 microM, 13.55 microM, 15.29 microM on HeLa cell line. Their activities are comparable with garcinol which is a cell permeable histone acetyltransferase (HAT) inhibitor and 10 fold more active than p300 HAT activators so far reported.

  10. Potential biological applications of bio-based anacardic acids and their derivatives.

    Science.gov (United States)

    Hamad, Fatma B; Mubofu, Egid B

    2015-04-16

    Cashew nut shells (CNS), which are agro wastes from cashew nut processing factories, have proven to be among the most versatile bio-based renewable materials in the search for functional materials and chemicals from renewable resources. CNS are produced in the cashew nut processing process as waste, but they contain cashew nut shell liquid (CNSL) up to about 30-35 wt. % of the nut shell weight depending on the method of extraction. CNSL is a mixture of anacardic acid, cardanol, cardol, and methyl cardol, and the structures of these phenols offer opportunities for the development of diverse products. For anacardic acid, the combination of phenolic, carboxylic, and a 15-carbon alkyl side chain functional group makes it attractive in biological applications or as a synthon for the synthesis of a multitude of bioactive compounds. Anacardic acid, which is about 65% of a CNSL mixture, can be extracted from the agro waste. This shows that CNS waste can be used to extract useful chemicals and thus provide alternative green sources of chemicals, apart from relying only on the otherwise declining petroleum based sources. This paper reviews the potential of anacardic acids and their semi-synthetic derivatives for antibacterial, antitumor, and antioxidant activities. The review focuses on natural anacardic acids from CNS and other plants and their semi-synthetic derivatives as possible lead compounds in medicine. In addition, the use of anacardic acid as a starting material for the synthesis of various biologically active compounds and complexes is reported.

  11. Gastroprotective Mechanisms of Action of Semisynthetic Carnosic Acid Derivatives in Human Cells

    Directory of Open Access Journals (Sweden)

    Cristina Theoduloz

    2014-01-01

    Full Text Available Carnosic acid (CA and its semisynthetic derivatives display relevant gastroprotective effects on HCl/ethanol induced gastric lesions in mice. However, little is known on the mechanisms of action of the new compounds. The aim of the present work was to assess the gastroprotective action mechanisms of CA and its derivatives using human cell culture models. A human gastric adenocarcinoma cell line (AGS and lung fibroblasts (MRC-5 were used to reveal the possible mechanisms involved. The ability of the compounds to protect cells against sodium taurocholate (NaT-induced damage, and to increase the cellular reduced glutathione (GSH and prostaglandin E2 (PGE2 content was determined using AGS cells. Stimulation of cell proliferation was studied employing MRC-5 fibroblasts. Carnosic acid and its derivatives 10–18 raised GSH levels in AGS cells. While CA did not increase the PGE2 content in AGS cells, all derivatives significantly stimulated PGE2 synthesis, the best effect being found for the 12-O-indolebutyrylmethylcarnosate 13. A significant increase in MRC-5 fibroblast proliferation was observed for the derivatives 7 and 16–18. The antioxidant effect of the compounds was assessed by the inhibition of lipid peroxidation in human erythrocyte membranes, scavenging of superoxide anion and DPPH discoloration assay. The new CA derivatives showed gastroprotective effects by different mechanisms, including protection against cell damage induced by NaT, increase in GSH content, stimulation of PGE2 synthesis and cell proliferation.

  12. Enzymatic synthesis of enantiopure alpha- and beta-amino acids by phenylalanine aminomutase-catalysed amination of cinnamic acid derivatives.

    Science.gov (United States)

    Wu, Bian; Szymanski, Wiktor; Wietzes, Piet; de Wildeman, Stefaan; Poelarends, Gerrit J; Feringa, Ben L; Janssen, Dick B

    2009-01-26

    The phenylalanine aminomutase (PAM) from Taxus chinensis catalyses the conversion of alpha-phenylalanine to beta-phenylalanine, an important step in the biosynthesis of the N-benzoyl phenylisoserinoyl side-chain of the anticancer drug taxol. Mechanistic studies on PAM have suggested that (E)-cinnamic acid is an intermediate in the mutase reaction and that it can be released from the enzyme's active site. Here we describe a novel synthetic strategy that is based on the finding that ring-substituted (E)-cinnamic acids can serve as a substrate in PAM-catalysed ammonia addition reactions for the biocatalytic production of several important beta-amino acids. The enzyme has a broad substrate range and a high enantioselectivity with cinnamic acid derivatives; this allows the synthesis of several non-natural aromatic alpha- and beta-amino acids in excellent enantiomeric excess (ee >99 %). The internal 5-methylene-3,5-dihydroimidazol-4-one (MIO) cofactor is essential for the PAM-catalysed amination reactions. The regioselectivity of amination reactions was influenced by the nature of the ring substituent.

  13. Detection and quantification of protein adduction by electrophilic fatty acids: mitochondrial generation of fatty acid nitroalkene derivatives.

    Science.gov (United States)

    Schopfer, F J; Batthyany, C; Baker, P R S; Bonacci, G; Cole, M P; Rudolph, V; Groeger, A L; Rudolph, T K; Nadtochiy, S; Brookes, P S; Freeman, B A

    2009-05-01

    Nitroalkene fatty acid derivatives manifest a strong electrophilic nature, are clinically detectable, and induce multiple transcriptionally regulated anti-inflammatory responses. At present, the characterization and quantification of endogenous electrophilic lipids are compromised by their Michael addition with protein and small-molecule nucleophilic targets. Herein, we report a trans-nitroalkylation reaction of nitro-fatty acids with beta-mercaptoethanol (BME) and apply this reaction to the unbiased identification and quantification of reaction with nucleophilic targets. Trans-nitroalkylation yields are maximal at pH 7 to 8 and occur with physiological concentrations of target nucleophiles. This reaction is also amenable to sensitive mass spectrometry-based quantification of electrophilic fatty acid-protein adducts upon electrophoretic resolution of proteins. In-gel trans-nitroalkylation reactions also permit the identification of protein targets without the bias and lack of sensitivity of current proteomic approaches. Using this approach, it was observed that fatty acid nitroalkenes are rapidly metabolized in vivo by a nitroalkene reductase activity and mitochondrial beta-oxidation, yielding a variety of electrophilic and nonelectrophilic products that could be structurally characterized upon BME-based trans-nitroalkylation reaction. This strategy was applied to the detection and quantification of fatty acid nitration in mitochondria in response to oxidative inflammatory conditions induced by myocardial ischemia-reoxygenation.

  14. Effect of root derived organic acids on the activation of nutrients in the rhizosphere soil

    Institute of Scientific and Technical Information of China (English)

    2002-01-01

    Four types of soils, including brown coniferous forest soil, dark brown soil, black soil, and black calic soil, sampled from three different places in northeast China were used in this test. The functions of two root-derived organic acids and water were simulated and compared in the activation of mineral nutrients from the rhizosphere soil. The results showed that the organic acids could activate the nutrients and the activated degree of the nutrient elements highly depended on the amount and types of the organic acid excreted and on the physiochemical and biochemical properties of the soil tested. The activation effect of the citric acid was obviously higher than that of malic acid in extracting Fe, Mn, Cu, and Zn for all the tested soil types. However, the activation efficiencies of P, K, Ca, and Mg extracting by the citric acid were not much higher, sometimes even lower, than those by malic acid. The solution concentration of all elements increased with increase of amount of the citric acid added.

  15. Differential diffusion effects on buoyancy-driven instabilities of acid-base fronts: the case of a color indicator.

    Science.gov (United States)

    Kuster, S; Riolfo, L A; Zalts, A; El Hasi, C; Almarcha, C; Trevelyan, P M J; De Wit, A; D'Onofrio, A

    2011-10-14

    Buoyancy-driven hydrodynamic instabilities of acid-base fronts are studied both experimentally and theoretically in the case where an aqueous solution of a strong acid is put above a denser aqueous solution of a color indicator in the gravity field. The neutralization reaction between the acid and the color indicator as well as their differential diffusion modifies the initially stable density profile in the system and can trigger convective motions both above and below the initial contact line. The type of patterns observed as well as their wavelength and the speed of the reaction front are shown to depend on the value of the initial concentrations of the acid and of the color indicator and on their ratio. A reaction-diffusion model based on charge balances and ion pair mobility explains how the instability scenarios change when the concentration of the reactants are varied.

  16. Folic acid derivatives for PET imaging and therapy addressing folate receptor positive tumors

    Energy Technology Data Exchange (ETDEWEB)

    Schieferstein, Hanno

    2013-07-01

    conducted. The synthesis of the folate-boron clusters was straightforward. At first, a linker molecule based on maleic acid was synthesized, which was coupled to the boron cluster via Michael Addition of a thiol and alkene and subsequently coupled to the targeting moiety using CuAAC. The new conjugates of folate and boron clusters led to a significant increase of boron concentration in the cell of about 5-times compared to currently used and approved boron pharmaceuticals. Moreover, azido-folate derivatives were coupled to macromolecular carrier systems (pHPMA), which showed an enhanced and specific accumulation at target sites (up to 2.5-times) during in vivo experiments. A specific blockade could be observed up to 30% indicating an efficient targeting effect. A new kind of nanoparticles consisting of a PDLLA core and p((HPMA)-b-(LMA)) as surfactants were developed and successfully radiolabeled via {sup 18}F-click chemistry in good RCYs of 8±3%. The nanoparticles were obtained via the miniemulsion technique in combination with solvent evaporation. The {sup 18}F-labeled nanoparticles were applied to in vivo testing using a mouse model. PET imaging showed a ''mixed'' biodistribution of low molecular weight as well as high molecular weight systems, indicating a partial loss of the {sup 18}F-labeled surfactant. In conclusion, the presented work successfully utilized the FR-targeting concept in both, the diagnostic field (PET imaging) and for therapeutic approaches (BNCT, drug delivery systems). As a result, the high potential of FR-targeting in oncological applications has been shown and was confirmed by small animal PET imaging.

  17. Scaleable production and separation of fermentation-derived acetic acid. Final CRADA report.

    Energy Technology Data Exchange (ETDEWEB)

    Snyder, S. W.; Energy Systems

    2010-02-08

    Half of U.S. acetic acid production is used in manufacturing vinyl acetate monomer (VAM) and is economical only in very large production plants. Nearly 80% of the VAM is produced by methanol carbonylation, which requires high temperatures and exotic construction materials and is energy intensive. Fermentation-derived acetic acid production allows for small-scale production at low temperatures, significantly reducing the energy requirement of the process. The goal of the project is to develop a scaleable production and separation process for fermentation-derived acetic acid. Synthesis gas (syngas) will be fermented to acetic acid, and the fermentation broth will be continuously neutralized with ammonia. The acetic acid product will be recovered from the ammonium acid broth using vapor-based membrane separation technology. The process is summarized in Figure 1. The two technical challenges to success are selecting and developing (1) microbial strains that efficiently ferment syngas to acetic acid in high salt environments and (2) membranes that efficiently separate ammonia from the acetic acid/water mixture and are stable at high enough temperature to facilitate high thermal cracking of the ammonium acetate salt. Fermentation - Microbial strains were procured from a variety of public culture collections (Table 1). Strains were incubated and grown in the presence of the ammonium acetate product and the fastest growing cultures were selected and incubated at higher product concentrations. An example of the performance of a selected culture is shown in Figure 2. Separations - Several membranes were considered. Testing was performed on a new product line produced by Sulzer Chemtech (Germany). These are tubular ceramic membranes with weak acid functionality (see Figure 3). The following results were observed: (1) The membranes were relatively fragile in a laboratory setting; (2) Thermally stable {at} 130 C in hot organic acids; (3) Acetic acid rejection > 99%; and (4

  18. The influence of the crystal structure on aggregation-induced luminescence of derivatives of aminobenzoic acid

    Science.gov (United States)

    Nosova, D. A.; Zarochentseva, E. P.; Vysotskaya, S. O.; Klemesheva, N. A.; Korotkov, V. I.

    2014-12-01

    The luminescence of three derivatives of 2-(phenylamino)-benzoic acid (N-phenylanthranilic, mefenamic, and niflumic acids) in benzene solution, in the polycrystalline state, and in the hexamethylbenzene matrix is studied. In the crystalline state, these compounds exhibit intense aggregation-induced luminescence. An increase in luminescence is also observed in the impurity crystal. The hexamethylbenzene crystal lattice restricts the mobility of molecules, thus ensuring the rigidity of the molecular structure of acids, which decreases the efficiency of nonradiative electron energy degradation. The main reason for the increase in the luminescence intensity in the case of fixation in a crystalline matrix is the formation of intramolecular hydrogen bonds and dimers of acid molecules.

  19. Chiral trans-1,2-diaminocyclohexane derivatives as chiral solvating agents for carboxylic acids

    Indian Academy of Sciences (India)

    Mariappan Periasamy; Manasi Dalai; Meduri Padmaja

    2010-07-01

    Efficient use of the readily accessible chiral 2-symmetric acyclic diamines (1-2) as well as macrocyclic amines (3-5) containing trans-1,2-diaminocyclohexyl moiety as chiral solvating agents (CSA) for the determination of enantiomeric excess of representative carboxylic acids (6-7) and an amino acid derivative (8) is illustrated. The enantiomeric composition of different carboxylic acids estimated here by the 1H NMR method, based on the integration of the corresponding methine proton signals are in good correlation with that determined using HPLC method. The data are in accordance with the formation of multimolecular diastereomeric complexes in solution, which render good splitting of NMR signals for the enantiomers of representative carboxylic acids as well as for -Ts-phenylglycine (up to = 0.295 ppm, 118 Hz).

  20. 2,5-PRODAN Derivatives as Highly Sensitive Sensors of Low Solvent Acidity

    Directory of Open Access Journals (Sweden)

    Alexandra H. Yoon

    2014-05-01

    Full Text Available Two 5-acyl-2-dimethylaminonaphthalene derivatives, one with a propionyl group and the other with a fused cyclohexanone ring, are investigated as sensors of H-bond-donating ability in protic solvents of low solvent acidity. Their fluorescence is highly quenched in protic solvents, and the quenching order of magnitude is linearly related to the H-bond-donating ability of the solvent as quantified by the solvent acidity (SA scale. As the solvent acidity increases from 0.15 to 0.40, the fluorescence for both is quenched by more than a factor of ten; thus, they are extremely sensitive sensors of the hydrogen-bond-donating ability in this weakly acidic range. Preferential solvation studies suggest that quenching occurs from a doubly H-bonded excited state.

  1. Two glucosylated abscisic acid derivates from avocado seeds (Persea americana Mill. Lauraceae cv. Hass).

    Science.gov (United States)

    del Refugio Ramos, María; Jerz, Gerold; Villanueva, Socorro; López-Dellamary, Fernando; Waibel, Reiner; Winterhalter, Peter

    2004-04-01

    Phytochemical investigation of avocado seed material (Persea americana Mill., Lauraceae) resulted in the isolation of two glucosylated abscisic acid derivates. One of these was not known as a natural product and can be regarded as a potential 'missing link' in abscisic acid metabolism in plants. After fractionation by high-speed countercurrent chromatography, and multiple steps of column chromatography, structures were elucidated by 1D-, 2D-NMR, electrospray-MS to be the novel beta-d-glucoside of (1'S,6'R)-8'-hydroxyabscisic acid, and (1'R,3'R,5'R,8'S)-epi-dihydrophaseic acid beta-d-glucoside. Absolute configuration was determined by circulardichroism, optical rotation, and by NOE experiments.

  2. Dienophile-Modified Mannosamine Derivatives for Metabolic Labeling of Sialic Acids: A Comparative Study.

    Science.gov (United States)

    Dold, Jeremias E G A; Pfotzer, Jessica; Späte, Anne-Katrin; Wittmann, Valentin

    2017-03-20

    Sialic acids play an important role in numerous cell adhesion processes and sialylation levels are known to be altered under certain pathogenic conditions such as cancer. Metabolic glycoengineering with mannosamine derivatives is a convenient way to introduce non-natural chemical reporter groups into sialylated glycoconjugates offering the opportunity to label sialic acids using bioorthogonal ligation chemistry. The labeling intensity not only depends on the rate of the ligation reaction but also on the extent to which the natural sialic acids are replaced by the modified ones, i.e. the incorporation efficiency. Here we present a comparative study of eight mannosamine derivatives featuring terminal alkenes as chemical reporter groups that can be labeled by an inverse-electron-demand Diels-Alder (DAinv) reaction. The derivatives differ in chain length as well as the type of linkage (comprising carbamates, amides, and a urea) that connects the terminal alkene to the sugar. As a general trend, increasing chain lengths result in higher DAinv reactivity and at the same time reduced incorporation efficiency. Carbamates are better accepted than amides with the same chain length; nevertheless do the latter result in more intense cell-surface staining visible in life-cell fluorescence microscopy. Finally, a urea derivative was shown to be accepted.

  3. Derivation of Nationally Consistent Indices Representing Urban Intensity Within and Across Nine Metropolitan Areas of the Conterminous United States

    Science.gov (United States)

    Cuffney, Thomas F.; Falcone, James A.

    2009-01-01

    Two nationally consistent multimetric indices of urban intensity were developed to support studies of the effects of urbanization on streams in nine metropolitan areas of the conterminous United States: Atlanta, Georgia; Birmingham, Alabama; Boston, Massachusetts; Dallas-Fort Worth, Texas; Denver, Colorado; Milwaukee-Green Bay, Wisconsin; Portland, Oregon; Raleigh, North Carolina; and Salt Lake City, Utah. These studies were conducted as a part of the U.S. Geological Survey's National Water-Quality Assessment Program. These urban intensity indices were used to define gradients of urbanization and to interpret biological, physical, and chemical changes along these gradients. Ninety census, land-cover, and infrastructure variables obtained from nationally available databases were evaluated. Only variables that exhibited a strong and consistent linear relation with 2000 population density were considered for use in the indices. Housing-unit density (HUDEN), percentage of basin area in developed land (P_NLCD1_2), and road density (ROADDEN) were selected as the best representatives of census, land-cover, and infrastructure variables. The metropolitan area national urban intensity index (MA-NUII) was scaled to represent urban intensity within each metropolitan area and ranged from 0 (little or no urban) to 100 (maximum urban) for sites within each metropolitan area. The national urban intensity index (NUII) was scaled to represent urban intensity across all nine metropolitan areas and ranged from 0 to 100 for all sites. The rates at which HUDEN, P_NLCD1_2, and ROADDEN changed with changes in population density varied among metropolitan areas. Therefore, these variables were adjusted to obtain a more uniform rate of response across metropolitan areas in the derivation of the NUII. The NUII indicated that maximum levels of urban intensity occurred in the West and Midwest rather than in the East primarily because small inner-city streams in eastern metropolitan areas are

  4. The influence of humic acids derived from earthworm-processed organic wastes on plant growth

    Energy Technology Data Exchange (ETDEWEB)

    Atiyeh, R.M.; Lee, S.; Edwards, C.A.; Arancon, N.Q.; Metzger, J.D. [Ohio State University, Columbus, OH (United States). Soil Ecology Lab.

    2002-08-01

    Some effects of humic acids, formed during the breakdown of organic wastes by earthworms (vermicomposting), on plant growth were evaluated. In the first experiment, humic acids were extracted from pig manure vermicompost using the classic alkali/acid fractionation procedure and mixed with a soilless container medium (Metro-Mix 360), to provide a range of 0, 50, 100, 150, 200, 250, 500, 1000, 2000 and 4000 mg of humate per kg of dry weight of container medium, and tomato seedlings were grown in the mixtures. In the second experiment, humates extracted from pig manure and food wastes vermicomposts were mixed with vermiculite to provide a range of 0, 50, 125, 250, 500, 1000 and 4000 mg of humate per kg of dry weight of the container medium, and cucumber seedlings were grown in the mixtures. Both tomato and cucumber seedlings were watered daily with a solution containing all nutrients required to ensure that any differences in growth responses were not nutrient-mediated. The incorporation of both types of vermicompost-derived humic acids, into either type of soilless plant growth media, increased the growth of tomato and cucumber plants significantly, in terms of plant heights, leaf areas, shoot and root dry weights. Plant growth increased with increasing concentrations of humic acids incorporated into the medium up to a certain proportion, but this differed according to the plant species, the source of the vermicompost, and the nature of the container medium. Plant growth tended to be increased by treatments of the plants with 50-500 mg/kg humic acids, but often decreased significantly when the concentrations of humic acids derived in the container medium exceeded 500-1000 mg/kg. These growth responses were most probably due to hormone-like activity of humic acids from the vermicomposts or could have been due to plant growth hormones adsorbed onto the humates. (author)

  5. Derivation of an amino acid similarity matrix for peptide:MHC binding and its application as a Bayesian prior

    Directory of Open Access Journals (Sweden)

    Sette Alessandro

    2009-11-01

    Full Text Available Abstract Background Experts in peptide:MHC binding studies are often able to estimate the impact of a single residue substitution based on a heuristic understanding of amino acid similarity in an experimental context. Our aim is to quantify this measure of similarity to improve peptide:MHC binding prediction methods. This should help compensate for holes and bias in the sequence space coverage of existing peptide binding datasets. Results Here, a novel amino acid similarity matrix (PMBEC is directly derived from the binding affinity data of combinatorial peptide mixtures. Like BLOSUM62, this matrix captures well-known physicochemical properties of amino acid residues. However, PMBEC differs markedly from existing matrices in cases where residue substitution involves a reversal of electrostatic charge. To demonstrate its usefulness, we have developed a new peptide:MHC class I binding prediction method, using the matrix as a Bayesian prior. We show that the new method can compensate for missing information on specific residues in the training data. We also carried out a large-scale benchmark, and its results indicate that prediction performance of the new method is comparable to that of the best neural network based approaches for peptide:MHC class I binding. Conclusion A novel amino acid similarity matrix has been derived for peptide:MHC binding interactions. One prominent feature of the matrix is that it disfavors substitution of residues with opposite charges. Given that the matrix was derived from experimentally determined peptide:MHC binding affinity measurements, this feature is likely shared by all peptide:protein interactions. In addition, we have demonstrated the usefulness of the matrix as a Bayesian prior in an improved scoring-matrix based peptide:MHC class I prediction method. A software implementation of the method is available at: http://www.mhc-pathway.net/smmpmbec.

  6. Efficient synthesis of 1-azadienes derived from alpha-aminoesters. Regioselective preparation of alpha-dehydroamino acids, vinylglycines, and alpha-amino acids.

    Science.gov (United States)

    Palacios, Francisco; Vicario, Javier; Aparicio, Domitila

    2006-09-29

    An efficient synthesis of 1-azadienes derived from alpha-aminoesters is achieved through an aza-Wittig reaction of phosphazenes with beta,gamma-unsaturated alpha-ketoesters. Regioselective 1,2-reduction of these functionalized 1-azadienes affords vinylglycine derivatives, while conjugative 1,4-reduction gives alpha-dehydroamino acid compounds. Reduction of both the carbon-carbon and the imine-carbon-nitrogen double bonds leads to the formation of alpha-amino acid derivatives.

  7. Production of ethoxylated fatty acids derived from Jatropha non-edible oil as a nonionic fat-liquoring agent.

    Science.gov (United States)

    El-Shattory, Y; Abo-Elwafa, Ghada A; Aly, Saadia M; Nashy, El-Shahat H A

    2012-01-01

    Natural fatty derivatives (oleochemicals) have been used as intermediate materials in several industries replacing the harmful and expensive petrochemicals. Fatty ethoxylates are one of these natural fatty derivatives. In the present work Jatropha fatty acids were derived from the non edible Jatropha oil and used as the fat source precursor. The ethoxylation process was carried out on the derived fatty acids using a conventional cheap catalyst (K₂CO₃) in order to obtain economically and naturally valuable non-ionic surfactants. Ethoxylation reaction was proceeded using ethylene oxide gas in the presence of 1 or 2% K₂CO₃ catalyst at 120 and 145°C for 5, 8 and 12 hours. The prepared products were evaluated for their chemical and physical properties as well as its application as non- ionic fat-liquoring agents in leather industry. The obtained results showed that the number of ethylene oxide groups introduced in the fatty acids as well as their EO% increased as the temperature and time of the reaction increased. The highest ethoxylation number was obtained at 145°C for 8 hr. Also, the prepared ethoxylated products were found to be effective fat-liquors with high HLB values giving stable oil in water emulsions. The fat-liquored leather led to an improvement in its mechanical properties such as tensile strength and elongation at break. In addition, a significant enhancement in the texture of the treated leather by the prepared fat-liquors as indicated from the scanning electron microscope (SEM) images was observed.

  8. Experimental and Molecular Dynamics Simulations for Investigating the Effect of Fatty Acid and Its Derivatives on Low Sulfur Diesel Lubricity

    Institute of Scientific and Technical Information of China (English)

    Luo Hui; Fan Weiyu; Li Yang; Zhao Pinhui; Nan Guozhi

    2013-01-01

    In this work, fatty acid and its derivatives were adopted as lubricity additives for low sulfur diesel. Tribological evaluation obtained from the High-Frequency Reciprocating Rig (HFRR) apparatus showed that the lubricating performance of the additives increased in the following order:stearic acid>glycol monopalmitate>stearyl alcohol>ethyl palmitate>cetyl ethyl ether. The adsorption behavior of the additives on Fe (110) surface and Fe2O3 (001) surface was investigated by mo-lecular dynamics (MD) simulations to verify their lubricity performance. The results suggested that adsorption energies of the additives on Fe (110) surface are determined by the van der Waals forces, while adsorptions on Fe2O3 (001) surface are signiifcantly attributed to the electrostatic attractive forces. Higher values of adsorption energy of the additives on Fe2O3 (001) surface indicate that the additive has more efifcient lubricity enhancing properties.

  9. Cobalt(II)-catalyzed 1,4-addition of organoboronic acids to activated alkenes: an application to highly cis-stereoselective synthesis of aminoindane carboxylic acid derivatives.

    Science.gov (United States)

    Chen, Min-Hsien; Mannathan, Subramaniyan; Lin, Pao-Shun; Cheng, Chien-Hong

    2012-11-19

    It all adds up: The 1,4-addition of organoboronic acids to activated alkenes catalyzed by [Co(dppe)Cl(2)] is described. A [3+2]-annulation reaction of ortho-iminoarylboronic acids with acrylates to give various aminoindane carboxylic acid derivatives with cis-stereoselectivity is also demonstrated (see scheme; dppe = 1,2-bis(diphenylphosphino)ethane).

  10. Highly efficient production of D-lactic acid from chicory-derived inulin by Lactobacillus bulgaricus.

    Science.gov (United States)

    Xu, Qianqian; Zang, Ying; Zhou, Jie; Liu, Peng; Li, Xin; Yong, Qiang; Ouyang, Jia

    2016-11-01

    Inulin is a readily available feedstock for cost-effective production of biochemicals. To date, several studies have explored the production of bioethanol, high-fructose syrup and fructooligosaccharide, but there are no studies regarding the production of D-lactic acid using inulin as a carbon source. In the present study, chicory-derived inulin was used for D-lactic acid biosynthesis by Lactobacillus bulgaricus CGMCC 1.6970. Compared with separate hydrolysis and fermentation processes, simultaneous saccharification and fermentation (SSF) has demonstrated the best performance of D-lactic acid production. Because it prevents fructose inhibition and promotes the complete hydrolysis of inulin, the highest D-lactic acid concentration (123.6 ± 0.9 g/L) with a yield of 97.9 % was obtained from 120 g/L inulin by SSF. Moreover, SSF by L. bulgaricus CGMCC 1.6970 offered another distinct advantage with respect to the higher optical purity of D-lactic acid (>99.9 %) and reduced number of residual sugars. The excellent performance of D-lactic acid production from inulin by SSF represents a high-yield method for D-lactic acid production from non-food grains.

  11. Comparison of inhibition effects of some benzoic acid derivatives on sheep heart carbonic anhydrase

    Science.gov (United States)

    Kiliç, Deryanur; Yildiz, Melike; Şentürk, Murat; Erdoǧan, Orhan; Küfrevioǧlu, Ömer Irfan

    2016-04-01

    Carbonic anhydrase (CA) is a family of metalloenzymes that requires Zn as a cofactor and catalyze the quick conversion of CO2 to HCO3- and H+. Inhibitors of the carbonic anhydrases (CAs) have medical usage of significant diseases such as glaucoma, epilepsy, gastroduodenal ulcers, acid-base disequilibria and neurological disorders. In the present study, inhibition of CA with some benzoic derivatives (1-6) were investigated. Sheep heart CA (shCA) enzyme was isolated by means of designed affinity chromatography gel (cellulose-benzyl-sulfanylamide) 42.45-fold in a yield of 44 % with 564.65 EU/mg. Purified shCA enzyme was used in vitro studies. In the studies, IC50 values were calculated for 3-aminobenzoic acid (1), 4-aminobenzoic acid (2), 2-hydroxybenzoic acid (3), 2-benzoylbenzoic acid (4), 2,3-dimethoxybenzoic acid (5), and 3,4,5-trimethoxybenzoic acid (6), showing the inhibition effects on the purified enzyme. Such molecules can be used as pioneer for discovery of novel effective CA inhibitors for medicinal chemistry applications.

  12. Simultaneous derivative spectrophotometric analysis of doxylamine succinate, pyridoxine hydrochloride and folic Acid in combined dosage forms.

    Science.gov (United States)

    Pathak, A; Rajput, S J

    2008-01-01

    Two UV spectrophotometric methods have been developed, based on first derivative spectrophotometry for simultaneous estimation of doxylamine succinate, pyridoxine hydrochloride, and folic acid in tablet formulations. In method I, the concentrations of these drugs were determined by using linear regression equation. Method II is also based on first derivative spectrophotometry however simultaneous equations (Vierdot's method) were derived on derivative spectra. The first derivative amplitudes at 270.0, 332.8 and 309.2 nm were utilized for simultaneous estimation of these drugs respectively by both methods. In both the methods, linearity was obtained in the concentration range 2.5-50 mug/ml, 1-40 mug/ml and 1-30 mug/ml for doxylamine succinate, pyridoxine hydrochloride, and folic acid respectively. The developed methods show best results in terms of linearity, accuracy, precision, LOD, LOQ and ruggedness for standard laboratory mixtures of pure drugs and marketed formulations. The common excipients and additives did not interfere in their determinations.

  13. Simultaneous derivative spectrophotometric analysis of doxylamine succinate, pyridoxine hydrochloride and folic acid in combined dosage forms

    Directory of Open Access Journals (Sweden)

    Pathak A

    2008-01-01

    Full Text Available Two UV spectrophotometric methods have been developed, based on first derivative spectrophotometry for simultaneous estimation of doxylamine succinate, pyridoxine hydrochloride, and folic acid in tablet formulations. In method I, the concentrations of these drugs were determined by using linear regression equation. Method II is also based on first derivative spectrophotometry however simultaneous equations (Vierdot′s method were derived on derivative spectra. The first derivative amplitudes at 270.0, 332.8 and 309.2 nm were utilized for simultaneous estimation of these drugs respectively by both methods. In both the methods, linearity was obtained in the concentration range 2.5-50 µg/ml, 1-40 µg/ml and 1-30 µg/ml for doxylamine succinate, pyridoxine hydrochloride, and folic acid respectively. The developed methods show best results in terms of linearity, accuracy, precision, LOD, LOQ and ruggedness for standard laboratory mixtures of pure drugs and marketed formulations. The common excipients and additives did not interfere in their determinations.

  14. Anticonvulsant and behavioral effects observed in mice following treatment with an ester derivative of ferulic acid: Isopentyl ferulate.

    Science.gov (United States)

    Machado, Keylla C; Oliveira, George Laylson S; Machado, Kátia C; Islam, Md Torequl; Junior, Antonio Luiz G; De Sousa, Damião P; Freitas, Rivelilson M

    2015-12-01

    The objective of this study was to evaluate the potential anticonvulsant effect of isopentyl ferulate, a new ester derived from ferulic acid in mice (Mus musculus) subjected to two models of induced seizures. According to the results obtained, the IF at doses of 25, 50 and 75 mg/kg (i.p.) showed protective effect against induced seizures by pilocarpine (400 mg/kg, i.p.) and pentylenetetrazole (70 mg/kg, i.p.). In the two animal models of seizures, the pretreatment of the IF (25, 50 and 75 mg/kg) with flumazenil blocked the anticonvulsant effect, suggesting that the mechanism of action of this ester derived of ferulic acid may be related to activity in the benzodiazepine-binding site of the GABAA receptor (γ-aminobutyric acid, type A). In addition to the anticonvulsant effect, behavioral changes as neurotoxicity indication were assessed by using the rota rod and open field tests. The results obtained showed that the IF (25, 50 and 75 mg/kg) does not induce significant changes in locomotor activity and motor coordination when compared with the control group, unlike the results presented by diazepam. Thus, these results demonstrate a new pharmacological knowledge of IF with potential application against epileptic seizures. However, further studies are needed to elucidate other neurobiological mechanisms underlying epilepsy.

  15. Conformational analysis: a tool for the elucidation of the antioxidant properties of ferulic acid derivatives in membrane models.

    Science.gov (United States)

    Anselmi, Cecilia; Centini, Marisanna; Andreassi, Marco; Buonocore, Anna; La Rosa, Caterina; Facino, Roberto Maffei; Sega, Alessandro; Tsuno, Fumi

    2004-09-03

    With the aim to search and design more effective and safe antioxidant molecules to be used as functional ingredients in cosmetic formulations for UV protection, we evaluated the antioxidant/radical scavenging activities of ferulic acid and of some alkyl ferulates in both acellular and cellular systems. Ferulic acid esters, equipotent as antioxidant in homogeneous phase, showed when tested in membranous systems (rat liver microsomes, rat erythrocytes) marked differences in antioxidant potency. The n-C(12) derivative was the most potent, followed by n-C(8), n-C(16) and branched C(8), and then by ferulic acid. A conformational study carried out by NMR and modelling, indicates that the different antioxidant activity of ferulates in membrane models is due to the different spatial conformation and arrangement of the side chain of the molecule, which governs the access and binding to the phospholipid bilayer, the modality of orientation of the scavenging/quenching nucleus (phenol moiety), and hence the overall antioxidant potency of the derivative. These results emphasize the need of analytical studies (NMR and molecular modelling) addressed to the knowledge of the conformational parameters in combination with conventional antioxidant testings for understanding the antioxidant behaviour of a molecule in a biological membrane/system.

  16. Inclusion Behavior of Dimer b-Cyclodextrin Bridged with Aspartic Acid Derivative

    Institute of Scientific and Technical Information of China (English)

    2001-01-01

    The b-cyclodextrin (CD) dimer bridged with aspartic acid (ASP) derivative, FITC-ASP(NH-b-CD)2 (Host, FITC=fluorescein-4-isothiocyanate), was synthesized. Fluorescence polarization study showed that the novel host formed an inclusion compound, [FITC-ASP(NH-b-CD)2]ATA, for which Kd was determined to be 5.0×10-6 mol/L by Beacon 2000 Analyzer, when ATA (Guest) = Adm-Trp-Arg-Arg-NH2 (Adm = 1-adamantanecarboxylic acid, Trp = tryptophan, Arg = arginine), where Kd is the dissociation constant in aqueous solution at 298 K.

  17. Potential antibacterial activity of coumarin and coumarin-3-acetic acid derivatives.

    Science.gov (United States)

    Chattha, Fauzia Anjum; Munawar, Munawar Ali; Nisa, Mehrun; Ashraf, Mohammad; Kousar, Samina; Arshad, Shafia

    2015-05-01

    Coumarin and coumarin-3-acetic acid derivatives were synthesized by reacting phenols with malic acid, ethyl acetoacetate and ethyl acetylsuccinate in appropriate reaction conditions. All synthesized compounds were subjected to test for their antimicrobial activities against variety of gram positive (Bacillus subtilis, Staphylococcus aureus) and gram negative bacterial stains (Shigella sonnei, Escherichia coli) by agar dilution method. Several of them exhibited appreciable good antibacterial activity against the different strains of gram positive and gram negative bacteria. These findings suggest a great potential of these compounds for screening and use as antibacterial agents for further studies with a battery of bacteria.

  18. Diverse bacterial PKS sequences derived from okadaic acid-producing dinoflagellates.

    Science.gov (United States)

    Perez, Roberto; Liu, Li; Lopez, Jose; An, Tianying; Rein, Kathleen S

    2008-05-22

    Okadaic acid (OA) and the related dinophysistoxins are isolated from dinoflagellates of the genus Prorocentrum and Dinophysis. Bacteria of the Roseobacter group have been associated with okadaic acid producing dinoflagellates and have been previously implicated in OA production. Analysis of 16S rRNA libraries reveals that Roseobacter are the most abundant bacteria associated with OA producing dinoflagellates of the genus Prorocentrum and are not found in association with non-toxic dinoflagellates. While some polyketide synthase (PKS) genes form a highly supported Prorocentrum clade, most appear to be bacterial, but unrelated to Roseobacter or Alpha-Proteobacterial PKSs or those derived from other Alveolates Karenia brevis or Crytosporidium parvum.

  19. A Benzoic Acid Derivative and Flavokawains from Piper species as Schistosomiasis Vector Controls

    Directory of Open Access Journals (Sweden)

    Ludmila N. Rapado

    2014-04-01

    Full Text Available The search of alternative compounds to control tropical diseases such as schistosomiasis has pointed to secondary metabolites derived from natural sources. Piper species are candidates in strategies to control the transmission of schistosomiasis due to their production of molluscicidal compounds. A new benzoic acid derivative and three flavokawains from Piper diospyrifolium, P. cumanense and P. gaudichaudianum displayed significant activities against Biomphalaria glabrata snails. Additionally, “in silico” studies were performed using docking assays and Molecular Interaction Fields to evaluate the physical-chemical differences among the compounds in order to characterize the observed activities of the test compounds against Biomphalaria glabrata snails.

  20. A benzoic acid derivative and flavokawains from Piper species as schistosomiasis vector controls.

    Science.gov (United States)

    Rapado, Ludmila N; Freitas, Giovana C; Polpo, Adriano; Rojas-Cardozo, Maritza; Rincón, Javier V; Scotti, Marcus T; Kato, Massuo J; Nakano, Eliana; Yamaguchi, Lydia F

    2014-04-23

    The search of alternative compounds to control tropical diseases such as schistosomiasis has pointed to secondary metabolites derived from natural sources. Piper species are candidates in strategies to control the transmission of schistosomiasis due to their production of molluscicidal compounds. A new benzoic acid derivative and three flavokawains from Piper diospyrifolium, P. cumanense and P. gaudichaudianum displayed significant activities against Biomphalaria glabrata snails. Additionally, "in silico" studies were performed using docking assays and Molecular Interaction Fields to evaluate the physical-chemical differences among the compounds in order to characterize the observed activities of the test compounds against Biomphalaria glabrata snails.

  1. Stability of vitamin C derivatives in topical formulations containing lipoic acid, vitamins A and E.

    Science.gov (United States)

    Segall, A I; Moyano, M A

    2008-12-01

    The stability of ascorbyl palmitate, sodium ascorbyl phosphate and magnesium ascorbyl phosphate in topical formulations was investigated by direct reverse phase high performance liquid chromatography after sample dilution with a suitable buffer - organic solvent mixture. Ascorbyl palmitate, sodium ascorbyl phosphate and magnesium ascorbyl phosphate are derivatives of ascorbic acid which differ in hydrolipophilic properties. They are widely used in cosmetic and pharmaceutical preparations. According to the results, ascorbyl esters showed significant differences: sodium ascorbyl phosphate and magnesium ascorbyl phosphate are more stable derivatives of vitamin C than ascorbyl palmitate and may be easily used in cosmetic products.

  2. Phase Transfer Catalyzed Synthesis of Thiosemicarbazide Derivatives of 2-ethoxybenzoic Acid

    Institute of Scientific and Technical Information of China (English)

    WEI; TaiBao

    2001-01-01

    A series of 1,4-disubstitued thiosemicarbazides and their related heterocyclic compounds have been found to possess important biological activities[1]. Some thiosemicarbazides have been found to be useful as herbicides, insecticides and plant-growth regulators [1]. In view of these and in continuation of our earlier work on the synthesis and biological activity of thiosemicarbaides derivatives [2], we now report a convenient and efficient method for the preparation of thiosemicarbazides derivatives of 2-ethoxybenzoic acid under the condition of solid-liquid phase transfer catalysis using PEG-400 as the catalyst.  ……

  3. Phase Transfer Catalyzed Synthesis of Thiosemicarbazide Derivatives of 2-ethoxybenzoic Acid

    Institute of Scientific and Technical Information of China (English)

    WEI TaiBao; ZHANG YouMing; WU JiaWei

    2001-01-01

    @@ A series of 1,4-disubstitued thiosemicarbazides and their related heterocyclic compounds have been found to possess important biological activities[1]. Some thiosemicarbazides have been found to be useful as herbicides, insecticides and plant-growth regulators [1]. In view of these and in continuation of our earlier work on the synthesis and biological activity of thiosemicarbaides derivatives [2], we now report a convenient and efficient method for the preparation of thiosemicarbazides derivatives of 2-ethoxybenzoic acid under the condition of solid-liquid phase transfer catalysis using PEG-400 as the catalyst.

  4. Structure-dependent effects of pyridine derivatives on mechanisms of intestinal fatty acid uptake: regulation of nicotinic acid receptor and fatty acid transporter expression.

    Science.gov (United States)

    Riedel, Annett; Lang, Roman; Rohm, Barbara; Rubach, Malte; Hofmann, Thomas; Somoza, Veronika

    2014-07-01

    Pyridines are widely distributed in foods. Nicotinic acid (NA), a carboxylated pyridine derivative, inhibits lipolysis in adipocytes by activation of the orphan NA receptor (HM74A) and is applied to treat hyperlipidemia. However, knowledge on the impact of pyridine derivatives on intestinal lipid metabolism is scarce. This study was performed to identify the structural determinants of pyridines for their effects on fatty acid uptake in enterocyte-like Caco-2 cells and to elucidate the mechanisms of action. The impact of 17 pyridine derivatives on fatty acid uptake was tested. Multiple regression analysis revealed the presence of a methyl group to be the structural determinant at 0.1 mM, whereas at 1 mM, the presence of a carboxylic group and the N-methylation presented further structural characteristics to affect the fatty acid uptake. NA, showing a stimulating effect on FA uptake, and N-methyl-4-phenylpyridinium (MPP), inhibiting FA uptake, were selected for mechanistic studies. Gene expression of the fatty acid transporters CD36, FATP2 and FATP4, and the lipid metabolism regulating transcription factors peroxisome proliferator-activated receptor (PPAR) α and PPARγ was up-regulated upon NA treatment. Caco-2 cells were demonstrated to express the low-affinity NA receptor HM74 of which the gene expression was up-regulated upon NA treatment. We hypothesize that the NA-induced fatty acid uptake might result from NA receptor activation and related intracellular signaling cascades. In contrast, MPP increased transepithelial electrical resistance. We therefore conclude that NA and MPP, both sharing the pyridine motif core, exhibit their contrary effects on intestinal FA uptake by activation of different mechanisms.

  5. Synthesis and Characterization of Some Trivalent and Tetravalent Derivatives of 2- Hydroxy-1-naphthoic Acid

    Directory of Open Access Journals (Sweden)

    Deepti Joshi

    2004-01-01

    Full Text Available The trivalent derivatives (B, Al, As, Sb & Fe and tetravalent derivatives (Si, Ti & Se of 2-hydroxy-1-naphthoic acid have been prepared by the interaction of their corresponding isopropoxide with letter in different molar ratio viz. 1:3 &1:4 in benzene medium. The prepared compounds generally obtained as coloured solids and amongst them those containing isopropoxy groups were found to be hygroscopic. All these compound were characterized by azeotrope and elemental analysis as well as by IR, PMR and mass spectral measurements. These spectral data have facilitated in elucidating the mode of bonding of the said metals and non-metals in these compounds with 2-hydroxy-1-naphthoic acid.

  6. Synthesis of Chiral 1,4-Disubstituted-1,2,3-Triazole Derivatives from Amino Acids

    Directory of Open Access Journals (Sweden)

    Morten Grøtli

    2009-12-01

    Full Text Available A versatile method for the synthesis of chiral 1,4-disubstituted-1,2,3-triazole derivatives starting from easily accessible naturally occurring D-or L-amino acids as chiral synthons is described. The amino acids were converted into azido alcohols, followed by copper catalyzed [3+2] cycloaddition reactions between the azido alcohols and methyl propiolate and subsequent ester aminolysis with primary and secondary amines furnished the target compounds, which were obtained in excellent yields with no racemization. Docking of selected target compounds shows that the chiral 1,4-disubstituted-1,2,3-triazoles derivatives has the potential of mimicking the binding mode of known purine analogues.

  7. Severe Acute Local Reactions to a Hyaluronic Acid-derived Dermal Filler.

    Science.gov (United States)

    Van Dyke, Susan; Hays, Geoffrey P; Caglia, Anthony E; Caglia, Michael

    2010-05-01

    Injectable fillers are normally well tolerated by patients with little or no adverse effects. The most common side effects include swelling, redness, bruising, and pain at the injection site. This report describes three cases in which patients injected with a hyaluronic acid-derived injectable filler that is premixed with lidocaine developed adverse reactions including persistent swelling, pain, and nodule formation. Two of the three patients' abscesses were cultured for aerobic and anaerobic bacteria and mycobacterium. All three cultures were negative. Abscess persistence in all cases necessitated physical removal and/or enzymatic degradation with hyaluronidase. The effects subsided only after the product had been removed. Two of these patients were subsequently treated with other hyaluronic acid-derived dermal fillers without adverse events.

  8. Stereoselective Synthesis of α-Amino-C-phosphinic Acids and Derivatives

    Directory of Open Access Journals (Sweden)

    José Luis Viveros-Ceballos

    2016-08-01

    Full Text Available α-Amino-C-phosphinic acids and derivatives are an important group of compounds of synthetic and medicinal interest and particular attention has been dedicated to their stereoselective synthesis in recent years. Among these, phosphinic pseudopeptides have acquired pharmacological importance in influencing physiologic and pathologic processes, primarily acting as inhibitors for proteolytic enzymes where molecular stereochemistry has proven to be critical. This review summarizes the latest developments in the asymmetric synthesis of acyclic and phosphacyclic α-amino-C-phosphinic acids and derivatives, following in the first case an order according to the strategy used, whereas for cyclic compounds the nitrogen embedding in the heterocyclic core is considered. In addition selected examples of pharmacological implications of title compounds are also disclosed.

  9. Synthetic studies of coumarin derivatives from o-hydroxybenzophenones with phenylacetic acid and acetic anhydride

    Energy Technology Data Exchange (ETDEWEB)

    Kang, Soon Hee; Yang, Sung Yun [Ewha Womans Univ., Seoul (Korea, Republic of)

    1999-02-01

    The 8 coumarin derivatives have been synthesized from 8 starting materials(2-hydroxy-benzophenone, 2,2'-dihydroxybenzophenone, 2,4-dihydroxybenzophenone, 2-hydroxy-5-methylbenzophenone, 5-chloro-2-hydroxy-4-methylbenzophenone, 2-hydroxy-4-methoxybenzophenone, 2-hydroxy-4-methoxybenzophenone, 2-hydroxy-4-4'-dimethoxybenzophenone) with phenylacetic acid and Ac{sub 2}O/TEA in acetone at reflux temperature. The ratio of o-hydroxybenzophenone, phenylacetic acid, Ac{sub 2}O and TEA is 1:1:8:8 in acetone. Our results showed higher products yields of coumarin derivatives than Shama and Ray's method in previous papers. A new intermediate form was proposed to our mechanism of coumarin synthetic method.

  10. HPLC Enantioseparation of Phenylcarbamic Acid Derivatives by Using Macrocyclic Chiral Stationary Phases

    Directory of Open Access Journals (Sweden)

    Hroboňová Katarína

    2016-06-01

    Full Text Available The HPLC by using chiral stationary phases based on macrocyclic antibiotics, dimethylphenyl carbamate cyklofructan 7 and β-cyclodextrin in terms of polar-organic separation mode (mobile phase methanol/acetonitrile/acetic acid/triethylamine were used for enantioseparation of alkoxy derivatives of phenylcarbamic acid. The effect of the analyte structures on the efficiency of enantioseparation was investigated. The most suitable stationary phase was teicoplanin aglycone, where the separations of the enantiomers were obtained (the resolution value from 0.65 to 2.90, depending on the structure of the analyte. Significant effect on the resolution of the enantiomers has position of alkoxy substituent in the hydrophobic part of the molecule. The enantiorecognition was achieved for 3-alkoxysubstituted derivatives.

  11. Synthesis and Preliminary Evaluation of the Antimicrobial Activity of Selected 3-Benzofurancarboxylic Acid Derivatives

    Directory of Open Access Journals (Sweden)

    Irena Wolska

    2010-07-01

    Full Text Available Halogen derivatives of selected 3-benzofurancarboxylic acids were prepared using 6-acetyl-5-hydroxy-2-methyl-3-benzofuranocarboxylic acid as starting material. 1H-NMR spectra were obtained for all of the synthesized structures, and for compound VI, an X-ray crystal structure was also obtained. All derivatives were tested for antimicrobial activity against a selection of Gram-positive cocci, Gram-negative rods and yeasts. Three compounds, III, IV, and VI, showed antimicrobial activity against Gram-positive bacteria (MIC 50 to 200 mg/mL. Compounds VI and III exhibited antifungal activity against the Candida strains C. albicans and C. parapsilosis (MIC – 100 mg/mL.

  12. Supramolecular chiral host-guest nanoarchitecture induced by the selective assembly of barbituric acid derivative enantiomers

    Science.gov (United States)

    Sun, Xiaonan; Silly, Fabien; Maurel, Francois; Dong, Changzhi

    2016-10-01

    Barbituric acid derivatives are prochiral molecules, i.e. they are chiral upon adsorption on surfaces. Scanning tunneling microscopy reveals that barbituric acid derivatives self-assemble into a chiral guest-host supramolecular architecture at the solid-liquid interface on graphite. The host nanoarchitecture has a sophisticated wavy shape pattern and paired guest molecules are nested insides the cavities of the host structure. Each unit cell of the host structure is composed of both enantiomers with a ratio of 1:1. Furthermore, the wavy patterns of the nanoarchitecture are formed from alternative appearance of left- and right-handed chiral building blocks, which makes the network heterochiral. The functional guest-host nanoarchitecture is the result of two-dimensional chiral amplification from single enantiomers to organizational heterochiral supramolecular self-assembly.

  13. Design and Synthesis of p/m-[p-(un)Substituted Phenylsulfonamido]phenyl β-Diketo Acids and Quinoxalone Derivatives

    Institute of Scientific and Technical Information of China (English)

    ZENG,Cheng-Chu; LI,Xue-Mei; YAN,Hong; ZHONG,Ru-Gang

    2007-01-01

    Diketo acid derivatives are potent and selective HIV-1 integrase inhibitors. To investigate the detailed synthesis of those derivatives, a series of p/m-[p-(un)substituted phenylsulfonamido]phenyl β-diketo acid derivatives have been designed and synthesized. The quinoxalone derivatives as the potential bioisosteres of the biologically labile β-diketoacid pharmacophores have also been synthesized from reactions of the corresponding diketo acids with o-phenylenediamine. The structures of all diketo acid (ester) and quinoxalone derivatives were confirmed by 1H NMR, 13C NMR, IR, HRMS and/or MS (ESI). X-ray crystallographic analysis of 11b demonstrates a similar arrangement of the side chain of quinoxalone derivatives with the parent diketoacids due to the intramolecular hydrogen bond (O…H-N) and the sp2 hybridization configuration of the two nitrogen atoms of the quinoxalone ring.

  14. Cyanide-insensitive and clofibrate enhanced beta-oxidation of dodecanedioic acid in rat liver. An indication of peroxisomal beta-oxidation of N-dicarboxylic acids.

    Science.gov (United States)

    Mortensen, P B; Kølvraa, S; Gregersen, N; Rasmussen, K

    1982-11-12

    The beta-oxidation rate of dodecanedioic acid in rat liver homogenates (600 X g supernatant fraction) was determined by simultaneous measurements of the C6-C12-dicarboxylic acids, i.e., adipic, suberic, sebacic and dodecanedioic acids, in relation to time in assays incubated with dodecanedioic acid. Measurements were performed by a combined gas chromatographic-mass spectrometric technique, i.e., selected ion-monitoring. The beta-oxidation rate was registered as the consumption rate of dodecanedioic acid and as the initial rise in the concentrations of C6-C10-dicarboxylic acids. The beta-oxidation rate of C8-C12-dicarboxylic acids was increased many times in homogenates from clofibrate-treated rats. Moreover, it was unexpectedly found that 2.0 mM cyanide was unable to inhibit the beta-oxidation rate of the dicarboxylic acids in vitro, but in fact caused a minor increase in the rate of beta-oxidation in homogenates from both normal and clofibrate-treated rats. It was concluded that the present results strongly indicate the existence of a peroxisomal beta-oxidation of dicarboxylic acids.

  15. Severe Acute Local Reactions to a Hyaluronic Acid-derived Dermal Filler

    OpenAIRE

    Van Dyke, Susan; Hays, Geoffrey P.; Caglia, Anthony E.; Caglia, Michael

    2010-01-01

    Injectable fillers are normally well tolerated by patients with little or no adverse effects. The most common side effects include swelling, redness, bruising, and pain at the injection site. This report describes three cases in which patients injected with a hyaluronic acid-derived injectable filler that is premixed with lidocaine developed adverse reactions including persistent swelling, pain, and nodule formation. Two of the three patients' abscesses were cultured for aerobic and anaerobic...

  16. Enzymatic Synthesis of Dipeptide Derivatives Containing Noncoded Amino Acids in Organic Solvents

    Institute of Scientific and Technical Information of China (English)

    YANG,Hong(杨洪); ZHOU,Chuang(周闯); TIAN,Gui-Ling(田桂玲); YE,Yun-Hua(叶蕴华)

    2002-01-01

    A series of dipeptide derivatives containing non-coded amino acis, N-Boc-4-X-Phe-Ala-NHNHNHPh (X= Cl, Br, I, NO2),were synthesized by using thermoase in organic solvents. The physical data were consistent with the same samples prepared by 3-( diethoxyphosphoryloxy)-1, 2, 3-benzotriazin-4 (3H)-one (DEPBT). Influence of different substituted groups of the non-coded amino acids and different organic solvents on the enzymatic peptide synthesis was studied.

  17. One-step synthesis of 1-chloro-3-arylacetone derivatives from arylacetic acids.

    Science.gov (United States)

    Zacuto, Michael J; Dunn, Robert F; Figus, Margaret

    2014-09-19

    A practical one-step method has been developed to prepare α-chloroketones from readily available, inexpensive phenylacetic acid derivatives. The method utilizes the unique reactivity of an intermediate Mg-enolate dianion, which displays selectivity for the carbonyl carbon of chloromethyl carbonyl electrophiles. Decarboxylation of the intermediate occurs spontaneously during the reaction quench. The utility of the reaction products has been demonstrated through the total synthesis of the natural product cimiracemate B.

  18. Heterogeneous and homogeneous catalysis for the hydrogenation of carboxylic acid derivatives: history, advances and future directions.

    Science.gov (United States)

    Pritchard, James; Filonenko, Georgy A; van Putten, Robbert; Hensen, Emiel J M; Pidko, Evgeny A

    2015-06-01

    The catalytic reduction of carboxylic acid derivatives has witnessed a rapid development in recent years. These reactions, involving molecular hydrogen as the reducing agent, can be promoted by heterogeneous and homogeneous catalysts. The milestone achievements and recent results by both approaches are discussed in this Review. In particular, we focus on the mechanistic aspects of the catalytic hydrogenation and highlight the bifunctional nature of the mechanism that is preferred for supported metal catalysts as well as homogeneous transition metal complexes.

  19. Bis(imidazolium) salts derived from amino acids as receptors and transport agents for chloride anions

    NARCIS (Netherlands)

    González-Mendoza, Laura; Altava, Belén; Burguete, M.I.; Escorihuela, Jorge; Hernando, Elsa; Luis, S.V.; Quesada, Roberto; Vicent, Cristian

    2015-01-01

    The binding properties of bis(imidazolium) hosts 1a-c derived from amino acids towards different anions have been studied by 1H NMR titration experiments in 95:05 CD3CN:H2O at 303 K, ESI-MS and theoretical calculations. Among this family, the salt 1c showed a stro

  20. Electrochemical Biosensors Based on Ferroceneboronic Acid and Its Derivatives: A Review

    Directory of Open Access Journals (Sweden)

    Baozhen Wang

    2014-07-01

    Full Text Available We review recent progress in the development of electrochemical biosensors based on ferroceneboronic acid (FcBA and ferrocene (Fc-modified boronic acids. These compounds can be used to construct electrochemical biosensors because they consist of a binding site (i.e., a boronic acid moiety and an electrochemically active part (i.e., an Fc residue. By taking advantage of the unique properties of FcBA and its derivatives, electrochemical sensors sensitive to sugars, glycated hemoglobin (HbA1c, fluoride (F− ions, and so forth have been widely studied. FcBA-based sugar sensors rely on the selective binding of FcBA to 1,2- or 1,3-diol residues of sugars through the formation of cyclic boronate ester bonds. The redox properties of FcBA-sugar adduct differ from those of free FcBA, which forms the basis of the electrochemical determination of sugars. Thus, non-enzymatic glucose sensors are now being actively studied using FcBA and Fc-modified boronic acids as redox markers. Using a similar principle, HbA1c can be detected by FcBA-based electrochemical systems because it contains hydrocarbon chains on the polypeptide chain. HbA1c sensors are useful for monitoring blood glucose levels over the preceding 8–12 weeks. In addition, FcBA and Fc-modified boronic acids have been used for the detection of F− ions due to the selective binding of boronic acid to F− ions. F−-ion sensors may be useful alternatives to conventional ion-selective electrodes sensitive to F− ion. Furthermore, FcBA derivatives have been studied to construct lectin; steroids; nucleotides; salicylic acid; and bacteria sensors. One of the limitations of FcBA-based sensors comes from the fact that FcBA derivatives are added in sample solutions as reagents. FcBA derivatives should be immobilized on the surface of electrodes for developing reagentless sensors.

  1. [Amino acid and peptide derivatives of the tylosin family of macrolide antibiotics modified at the aldehyde group].

    Science.gov (United States)

    Sumbatian, N V; Kuznetsova, I V; Karpenko, V V; Fedorova, N V; Chertkov, V A; Korshunova, G A; Bogdanov, A A

    2010-01-01

    Fourteen new functionally active amino acid and peptide derivatives of the antibiotics tylosin, desmycosin, and 5-O-mycaminosyltylonolide were synthesized in order to study the interaction of the growing polypeptide chain with the ribosomal tunnel. The conjugation of various amino acids and peptides with a macrolide aldehyde group was carried out by two methods: direct reductive amination with the isolation of the intermediate Schiff bases or through binding via oxime using the preliminarily obtained derivatives of 2-aminooxyacetic acid.

  2. Library of Antifouling Surfaces Derived From Natural Amino Acids by Click Reaction.

    Science.gov (United States)

    Xu, Chen; Hu, Xin; Wang, Jie; Zhang, Ye-Min; Liu, Xiao-Jiu; Xie, Bin-Bin; Yao, Chen; Li, Yi; Li, Xin-Song

    2015-08-12

    Biofouling is of great concern in numerous applications ranging from ophthalmological implants to catheters, and from bioseparation to biosensors. In this report, a general and facile strategy to combat surface fouling is developed by grafting of amino acids onto polymer substrates to form zwitterionic structure through amino groups induced epoxy ring opening click reaction. First of all, a library of poly(2-hydroxyethyl methacrylate-co-glycidyl methacrylate) hydrogels with zwitterionic surfaces were prepared, resulting in the formation of pairs of carboxyl anions and protonated secondary amino cations. The analysis of attenuated total reflectance Fourier transform infrared spectroscopy and X-ray photoelectron spectroscopy confirmed the successful immobilization of amino acids on the hydrogel surfaces. After that, the contact angle and equilibrium water content of the modified hydrogels showed that the hydrogels exhibited improved hydrophilicity compared with the parent hydrogel. Furthermore, the protein deposition was evaluated by bicinchoninic acid assay using bovine serum albumin (BSA) and lysozyme as models. The results indicated that the performance of the hydrogels was determined by the nature of incorporated amino acid: the hydrogels incorporated with neutral amino acids had nonspecific antiadsorption capability to both BSA and lysozyme; the hydrogels incorporated with charged amino acids showed antiadsorption behaviors against protein with same charge and enhanced adsorption to the protein with opposite charge; the optimal antiadsorption performance was observed on the hydrogels incorporated with polar amino acids with a hydroxyl residual. The improvement of antiprotein fouling of the neutral amino acids grafted hydrogels can be ascribed to the formation of zwitterionic surfaces. Finally, a couple of soft contact lenses grafted with amino acids were fabricated having improved antifouling property and hydrophilicity. The result demonstrated the success of

  3. Disinfection efficiency of peracetic acid (PAA): inactivation of coliphages and bacterial indicators in a municipal wastewater plant.

    Science.gov (United States)

    Zanetti, F; De Luca, G; Sacchetti, R; Stampi, S

    2007-11-01

    The aim of the study was to assess the efficiency of low doses of peracetic acid against viral and bacterial indicators in wastewater and to evaluate if the treatment allows regulatory requirements to be satisfied. A total of 31 samplings were carried out, each involving the collection of secondary effluent and of effluent disinfected with 1.2 or 1.5 mg l(-1) of peracetic acid (contact time 20 minutes). In each sample were measured: somatic coliphages, F-specific RNA bacteriophages, Escherichia coli, total and faecal coliforms, enterococci. Peracetic acid disinfection showed significant differences between the reductions of the microorganisms tested: E. coli showed the highest reduction (1.78 and 2.43 Log respectively with 1.2 and 1.5 mg l(-1) of peracetic acid) and phages the lowest (ranging between 0.52 and 0.60 Log). Only a concentration of 1.5 mg l(-1) of peracetic acid would enable the effluent to be discharged into surface waters in compliance with Italian regulations. The variability of microbial resistance against the peracetic acid disinfection treatment, underlines the importance of assessing disinfection efficiency by using more than one indicator microorganism. The detection of E. coli could be usefully accompanied by tests for more resistant microorganisms such as enterococci or coliphages. In conclusion, peracetic acid can be used for the disinfection of effluents even at low doses, with the advantage of reducing costs and preventing the formation of significant amounts of genotoxic by-products.

  4. Periconceptional bread intakes indicate New Zealand's proposed mandatory folic acid fortification program may be outdated: results from a postpartum survey

    Directory of Open Access Journals (Sweden)

    Mallard Simonette R

    2012-02-01

    Full Text Available Abstract Background In September 2009, a folic acid fortification mandate (135 μg/100 g bread was to be implemented in New Zealand. However, due to political and manufacturer objection, fortification was deferred until May 2012. Based on estimates of bread consumption derived from a 1997 nationally representative survey, this program was intended to deliver a mean additional intake of 140 μg folic acid/d to women of childbearing age. Little is known about current bread consumption patterns in this target group. The aim of this study was to assess bread consumption among women prior to and during pregnancy with the intent to estimate periconceptional folic acid intakes that would be derived from bread if mandatory fortification were implemented as currently proposed. Methods A retrospective survey of 723 postpartum women in hospitals and birthing centres across New Zealand was conducted using a self-administered questionnaire on bread intake prior to and during pregnancy and maternal socio-demographic and obstetric characteristics. Results Median bread intake before conception (2 slices/d was below that of previous data upon which the current fortification proposal was modeled (3-4 slices/d. If mandatory fortification is implemented as proposed, only 31% (95% CI = 24%-37% of childbearing-age women would attain an additional folic acid intake of ≥ 140 μg/d, with a mean of 119 μg/d (95% CI = 107 μg/d-130 μg/d. Based on these data, a fortification level of 160 μg/100 g bread is required to achieve the targeted mean of 140 μg folic acid/d. Nonetheless, under the current proposal additional folic acid intakes would be greatest among the least advantaged segments of the target population: Pacific and indigenous Māori ethnic groups; those with increased parity, lower income and education; younger and single mothers; and women with unplanned pregnancies. Subgroups predicted to derive less than adequate folic acid intakes from the proposed

  5. Metabolic engineering of Saccharomyces cerevisiae for production of fatty acid-derived biofuels and chemicals.

    Science.gov (United States)

    Runguphan, Weerawat; Keasling, Jay D

    2014-01-01

    As the serious effects of global climate change become apparent and access to fossil fuels becomes more limited, metabolic engineers and synthetic biologists are looking towards greener sources for transportation fuels. In recent years, microbial production of high-energy fuels by economically efficient bioprocesses has emerged as an attractive alternative to the traditional production of transportation fuels. Here, we engineered the budding yeast Saccharomyces cerevisiae to produce fatty acid-derived biofuels and chemicals from simple sugars. Specifically, we overexpressed all three fatty acid biosynthesis genes, namely acetyl-CoA carboxylase (ACC1), fatty acid synthase 1 (FAS1) and fatty acid synthase 2 (FAS2), in S. cerevisiae. When coupled to triacylglycerol (TAG) production, the engineered strain accumulated lipid to more than 17% of its dry cell weight, a four-fold improvement over the control strain. Understanding that TAG cannot be used directly as fuels, we also engineered S. cerevisiae to produce drop-in fuels and chemicals. Altering the terminal "converting enzyme" in the engineered strain led to the production of free fatty acids at a titer of approximately 400 mg/L, fatty alcohols at approximately 100mg/L and fatty acid ethyl esters (biodiesel) at approximately 5 mg/L directly from simple sugars. We envision that our approach will provide a scalable, controllable and economic route to this important class of chemicals.

  6. Assessing the Left Ventricular Systolic Function at the Bedside: The Role of Transpulmonary Thermodilution-Derived Indices

    Directory of Open Access Journals (Sweden)

    Gerardo Aguilar

    2011-01-01

    Full Text Available Evaluating the systolic function of the left ventricle (LV is important in the hemodynamic management of the critically ill patients with circulatory failure. Echocardiography is considered the standard monitor for estimating the LV function at the bedside in the intensive care unit. However, it requires a trained operator and is not a real-time monitoring tool. For monitoring of the systolic function, the pulmonary artery catheter has been the gold standard for a long time. However, now there are alternatives to this device, with transpulmonary thermodilution being one of them. This paper provides an overview of the usefulness of the transpulmonary thermodilution-derived indices for assessing systolic function at the bedside.

  7. A New Nanocatalytic Spectrophotometric Assay for Cationic Surfactant Using Phosphomolybdic Acid-Formic Acid-Nanogold as Indicator Reaction%A New Nanocatalytic Spectrophotometric Assay for Cationic Surfactant Using Phosphomolybdic Acid-Formic Acid-Nanogold as Indicator Reaction

    Institute of Scientific and Technical Information of China (English)

    蒋治良; 覃惠敏; 梁爱惠

    2012-01-01

    In the pH 7.4 Na2HPO4-NaH2PO4 buffer solution, the cationic surfactant (CS) interacted with nanogold particles (NG) to form NG aggregations (NGA) that resulted in its color changing from wine red to blue-violet. NG has a strong catalysis on the formic acid-phosphomolybdic acid (PMo) colored reaction, but that of the NGA catalysis is weak. With the increase of CS concentration, the NGA increased and the NG decreased, the catalysis decreased and the absorption value at 700 nm decreased linearly. The concentrations of 6.25-250 nmol/L tetradecyl dimethyl benzyl ammonium chloride (TDBAC), 0.625-250 nmol/L cetyltrimethyl ammonium bromide (CTMAB) and 12.5 -500 nmol-L 1 dodecyldimethylbenzyl ammonium chloride (DDBAC) had good linear responses to the decreased absorption value (AA70o nm), with molar absorption coefficients of 2.2 × 106, 2.1 × 106 and 9 ×105 Lomol 1.cm 1 respectively. This method was simple, highly sensitive and low-cost.

  8. Semi-Batch Deoxygenation of Canola- and Lard-Derived Fatty Acids to Diesel-Range Hydrocarbons

    Energy Technology Data Exchange (ETDEWEB)

    Ford, JP; Thapaliya, N; Kelly, MJ; Roberts, WL; Lamb, HH

    2013-12-01

    Fatty acids (FAs) derived via thermal hydrolysis of food-grade lard and canola oil were deoxygenated in the liquid phase using a commercially available 5 wt % Pd/C catalyst. Online quadrupole mass spectrometry and gas chromatography were used to monitor the effluent gases from the semi-batch stirred autoclave reactors. Stearic, oleic, and palmitic acids were employed as model compounds. A catalyst lifetime exceeding 2200 turnovers for oleic acid deoxygenation was demonstrated at 300 degrees C and 15 atm under 10% H-2. The initial decarboxylation rate of palmitic acid under 5% H-2 decreases sharply with increasing initial concentration; in contrast, the initial decarbonylation rate increases linearly, indicative of first-order kinetics. Scale-up of diesel-range hydrocarbon production was investigated by increasing the reactor vessel size, initial FA concentration, and FA/catalyst mass ratio. Lower CO2 selectivity and batch productivity were observed at the larger scales (600 and 5000 mL), primarily because of the higher initial FA concentration (67 wt %) employed. Because unsaturated FAs must be hydrogenated before deoxygenation can proceed at an appreciable rate, the additional batch time required for FA hydrogenation reduces the batch productivity for unsaturated feedstocks. Low-temperature hydrogenation of unsaturated feedstocks (using Pd/C or another less-expensive catalyst) prior to deoxygenation is recommended.

  9. Omega-3 fatty acids and cytochrome P450-derived eicosanoids in cardiovascular diseases: Which actions and interactions modulate hemodynamics?

    Science.gov (United States)

    Bonafini, Sara; Fava, Cristiano

    2017-01-01

    Increasing interest is focused on omega-3 fatty acids (FA) because of their potential beneficial effects, particularly in cardiovascular disease prevention. Eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA), two major omega-3 FA, are mainly consumed through diet, particularly from fish and seafood intake, whereas alpha-linolenic acid (ALA) is present in high amounts in leafy green vegetables, nuts and seeds. The hypothesis of a cardiovascular protective action of omega-3 FA derives mainly from observational studies, whereas the evidence from interventional studies is not always consistent. Nonetheless, clinical trials and meta-analyses indicate a positive action, at minimum on blood pressure (BP). Omega-3 FA may act through different biological pathways; however, in our review, we seek to revisit, most notably, the role of their metabolites via cytochrome P450 (CYP450) in hemodynamic modulation. We emphasize that the effect of omega-3 FA may depend on their balance with other dietary compounds, particularly omega-6 FA, which compete for the same pathways, thus modulating the production of metabolites. Furthermore, the biological activity of omega-3 FA might be better explained by the complex balance and interactions between a variety of nutrients and polymorphisms of genes implicated in specific metabolic pathways.

  10. Preparation and structural characterisation of novel and versatile amphiphilic octenyl succinic anhydride-modified hyaluronic acid derivatives

    DEFF Research Database (Denmark)

    Eenschooten, Corinne Diane; Guillaumie, Fanny; Kontogeorgis, Georgios

    2010-01-01

    The purpose of the present study was to prepare amphiphilic hyaluronic acid (HA) derivatives and to study the influence of a selection of reaction parameters on the degree of substitution (DS) of the derivatives. Octenyl succinic anhydride (OSA)–modified HA (OSA–HA) derivatives were prepared...

  11. A New Oleanolic Acid Derivative against CCl4-Induced Hepatic Fibrosis in Rats

    Directory of Open Access Journals (Sweden)

    Hongjun Xiang

    2017-03-01

    Full Text Available A novel hepatoprotective oleanolic acid derivative, 3-oxours-oleana-9(11, 12-dien-28-oic acid (Oxy-Di-OA, has been reported. In previous studies, we found that Oxy-Di-OA presented the anti-HBV (Hepatitis B Virus activity (IC50 = 3.13 µg/mL. Remarkably, it is superior to lamivudine in the inhibition of the rebound of the viral replication rate. Furthermore, Oxy-Di-OA showed good performance of anti-HBV activity in vivo. Some studies showed that liver fibrosis may affiliate with HBV gene mutations. In addition, the anti-hepatic fibrosis activity of Oxy-Di-OA has not been studied. Therefore, we evaluated the protective effect of Oxy-Di-OA against carbon tetrachloride (CCl4-induced liver injury in rats. Daily intraperitoneally administration of Oxy-Di-OA prevented the development of CCl4-induced liver fibrosis, which was evidenced by histological study and immunohistochemical analysis. The entire experimental protocol lasted nine weeks. Oxy-Di-OA significantly suppressed the increases of plasma aspartate aminotransferase (AST and alanine aminotransferase (ALT levels (p < 0.05. Furthermore, Oxy-Di-OA could prevent expression of transforming growth factor β1 (TGF-β1. It is worth noting that the high-dose group Oxy-Di-OA is superior to bifendate in elevating hepatic function. Compared to the model group, Oxy-Di-OA in the high-dose group and low-dose group can significantly reduce the liver and spleen indices (p < 0.05. The acute toxicity test showed that LD50 and a 95% confidence interval (CIs value of Oxy-Di-OA were 714.83 mg/kg and 639.73–798.73 mg/kg via intraperitoneal injection in mice, respectively. The LD50 value of Oxy-Di-OA exceeded 2000 mg/kg via gavage in mice. In addition, a simple and rapid high performance liquid chromatography-ultraviolet (HPLC-UV method was developed and validated to study the pharmacokinetic characteristics of the compound. After single-dose oral administration, time to reach peak concentration of Oxy-Di-OA (Cmax

  12. Brain-derived neurotrophic factor as an indicator of chemical neurotoxicity: an animal-free CNS cell culture model.

    Science.gov (United States)

    Woehrling, Elizabeth K; Hill, Eric J; Nagel, David; Coleman, Michael D

    2013-12-01

    Recent changes to the legislation on chemicals and cosmetics testing call for a change in the paradigm regarding the current 'whole animal' approach for identifying chemical hazards, including the assessment of potential neurotoxins. Accordingly, since 2004, we have worked on the development of the integrated co-culture of post-mitotic, human-derived neurons and astrocytes (NT2.N/A), for use as an in vitro functional central nervous system (CNS) model. We have used it successfully to investigate indicators of neurotoxicity. For this purpose, we used NT2.N/A cells to examine the effects of acute exposure to a range of test chemicals on the cellular release of brain-derived neurotrophic factor (BDNF). It was demonstrated that the release of this protective neurotrophin into the culture medium (above that of control levels) occurred consistently in response to sub-cytotoxic levels of known neurotoxic, but not non-neurotoxic, chemicals. These increases in BDNF release were quantifiable, statistically significant, and occurred at concentrations below those at which cell death was measureable, which potentially indicates specific neurotoxicity, as opposed to general cytotoxicity. The fact that the BDNF immunoassay is non-invasive, and that NT2.N/A cells retain their functionality for a period of months, may make this system useful for repeated-dose toxicity testing, which is of particular relevance to cosmetics testing without the use of laboratory animals. In addition, the production of NT2.N/A cells without the use of animal products, such as fetal bovine serum, is being explored, to produce a fully-humanised cellular model.

  13. SYNTHESIS AND ANTIBACTERIAL ACTIVITY OF SCHIFF BASE DERIVATIVES OF 4-CHLORO-3-NITROBENZOIC ACID

    Directory of Open Access Journals (Sweden)

    Kumari Santosh

    2012-12-01

    Full Text Available 4-chloro-3-nitrobenzoic acid was selected as nucleus structure having good antibacterial property. It was thought worthwhile to synthesize Schiff base derivatives of 4-chloro-3-nitrobenzoic acid in search of better antibacterial agents. The compounds were synthesized by first reducing nitro group in presence of Sn/HCl to 3-amino-4-chlorobenzoic acid, which on treatment with substituted benzaldehyde afforded the synthesis of the envisaged compounds. The synthesized compounds were purified and chemically characterized. They were screened for their antibacterial activity and result suggested that SKY-1, SKY-5 and SKY-8 were highly active against both Gram (+ and Gram(- bacteria like B.subtilis, S.aureus and E.coli whereas all are were found moderately to inactive against P.aeruginosa.

  14. Hybrid Compounds Strategy in the Synthesis of Oleanolic Acid Skeleton-NSAID Derivatives

    Directory of Open Access Journals (Sweden)

    Anna Pawełczyk

    2016-04-01

    Full Text Available The current study focuses on the synthesis of several hybrid individuals combining a natural oleanolic acid skeleton and synthetic nonsteroidal anti-inflammatory drug moieties (NSAIDs. It studied structural modifications of the oleanolic acid structure by use of the direct reactivity of hydroxyl or hydroxyimino groups at position C-3 of the triterpenoid skeleton with the carboxylic function of anti-inflammatory drugs leading to new perspective compounds with high potential pharmacological activities. Novel ester- and iminoester-type derivatives of oleanolic unit with the different NSAIDs, such as ibuprofen, aspirin, naproxen, and ketoprofen, were obtained and characterized. Moreover, preliminary research of compounds obtaining structure stability under acidic conditions was examined and the PASS method of prediction of activity spectra for substances was used to estimate the potential biological activity of these compounds.

  15. Synthesis and biological evaluation of sophocarpinic acid derivatives as anti-HCV agents

    Directory of Open Access Journals (Sweden)

    Yinghong Li

    2014-08-01

    Full Text Available Chronic hepatitis C virus (HCV infection has become a major public health burden worldwide. Twenty-two sophocarpinic acid or matrine derivatives were synthesized and their anti-HCV activities were evaluated in vitro. The structure-activity analysis revealed that (i sophocarpinic acids with a D-seco 3-ring structure scaffold were more favorable than matrines with a 4-ring scaffold; (ii the introduction of an electron-withdrawing group on the phenyl ring in 12-N-benzenesulfonyl Δβγ sophocarpinic acids was beneficial for the antiviral activity against HCV. Among them, compounds 9h and 9j exhibited the most potent inhibitory activities on HCV replication with selectivity indies of 70.3 and 30.9, respectively. Therefore, both were selected as antiviral candidates for further investigation.

  16. Synthesis and pharmacology of N-alkylated derivatives of the excitotoxin ibotenic acid.

    Science.gov (United States)

    Madsen, U; Dumpis, M A; Bräuner-Osborne, H; Piotrovsky, L B

    1998-06-16

    Three amino-alkylated derivatives of the naturally occurring excitatory amino acid (EAA) receptor agonist ibotenic acid (Ibo) have been synthesized and tested pharmacologically. N-Methyl-Ibo (1a) and N-ethyl-Ibo (1b) were shown to be agonists at NMDA receptors (EC50 = 140 and 320 microM, respectively), though with activities considerably lower than Ibo (EC50 = 9.6 microM). N-Benzyl-Ibo (1c) was inactive at ionotropic EAA receptors and all three compounds were, in contrast to Ibo, inactive at metabotropic EAA receptors. Molecular mechanics calculations have been performed on Ibo, 1a-c and the potent NMDA agonist 2-amino-2-(3-hydroxy-5-methyl-4-isoxazolyl)acetic acid (AMAA) in order to elucidate the observed structure-activity data.

  17. Synthesis and Cytotoxic Activity on Human Cancer Cells of Novel Isoquinolinequinone-Amino Acid Derivatives.

    Science.gov (United States)

    Valderrama, Jaime A; Delgado, Virginia; Sepúlveda, Sandra; Benites, Julio; Theoduloz, Cristina; Buc Calderon, Pedro; Muccioli, Giulio G

    2016-09-08

    A variety of aminoisoquinoline-5,8-quinones bearing α-amino acids moieties were synthesized from 3-methyl-4-methoxycarbonylisoquinoline-5,8-quinone and diverse l- and d-α-amino acid methyl esters. The members of the series were evaluated for their cytotoxic activity against normal and cancer cell lines by using the (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) (MTT) assay. From the current investigation, structure-activity relationships demonstrate that the location and structure of the amino acid fragment plays a significant role in the cytotoxic effects. Moderate to high cytotoxic activity was observed and four members, derived from l-alanine, l-leucine, l-phenylalanine, and d-phenylalanine, were selected as promising compounds by their IC50 ranging from 0.5 to 6.25 μM and also by their good selectivity indexes (≥2.24).

  18. Quantitative structure-activity relationships of antimicrobial fatty acids and derivatives against Staphylococcus aureus

    Institute of Scientific and Technical Information of China (English)

    Hui ZHANG; Lu ZHANG; Li-juan PENG; Xiao-wu DONG; Di WU; Vivian Chi-Hua WU; Feng-qin FENG

    2012-01-01

    Fatty acids and derivatives (FADs) are resources for natural antimicrobials.In order to screen for additional potent antimicrobial agents,the antimicrobial activities of FADs against Staphylococcus aureus were examined using a microplate assay.Monoglycerides of fatty acids were the most potent class of fatty acids,among which monotridecanoin possessed the most potent antimicrobial activity.The conventional quantitative structure-activity relationship (QSAR) and comparative molecular field analysis (CoMFA) were performed to establish two statistically reliable models (conventional QSAR:R2=0.942,Q2LOO=0.910; CoMFA:R2=0.979,Q2=0.588,respectively).Improved forecasting can be achieved by the combination of these two models that provide a good insight into the structureactivity relationships of the FADs and that may be useful to design new FADs as antimicrobial agents.

  19. Hydroxycinnamic Acids and Their Derivatives: Cosmeceutical Significance, Challenges and Future Perspectives, a Review

    Directory of Open Access Journals (Sweden)

    Oludemi Taofiq

    2017-02-01

    Full Text Available Bioactive compounds from natural sources, due to their widely-recognized benefits, have been exploited as cosmeceutical ingredients. Among them, phenolic acids emerge with a very interesting potential. In this context, this review analyzes hydroxycinnamic acids and their derivatives as multifunctional ingredients for topical application, as well as the limitations associated with their use in cosmetic formulations. Hydroxycinnamic acids and their derivatives display antioxidant, anti-collagenase, anti-inflammatory, antimicrobial and anti-tyrosinase activities, as well as ultraviolet (UV protective effects, suggesting that they can be exploited as anti-aging and anti-inflammatory agents, preservatives and hyperpigmentation-correcting ingredients. Due to their poor stability, easy degradation and oxidation, microencapsulation techniques have been employed for topical application, preventing them from degradation and enabling a sustained release. Based on the above findings, hydroxycinnamic acids present high cosmetic potential, but studies addressing the validation of their benefits in cosmetic formulations are still scarce. Furthermore, studies dealing with skin permeation are scarcely available and need to be conducted in order to predict the topical bioavailability of these compounds after application.

  20. Optical and thermal properties of azo derivatives of salicylic acid thin films

    Science.gov (United States)

    Ghoneim, M. M.; El-Ghamaz, N. A.; El-Sonbati, A. Z.; Diab, M. A.; El-Bindary, A. A.; Serag, L. S.

    2015-02-01

    N-acryloyl-4-aminosalicylic acid (4-AMSA), monomer (HL) and 5-(4‧-alkyl phenylazo)-N-acryloyl-4-aminosalicylic acid (HLn) are synthesized and characterized with various physico-chemical techniques. Thin films of 5-(4‧-alkyl phenylazo)-N-acryloyl-4-aminosalicylic acid (HLn) are prepared by spin coating technique. The X-ray diffraction (XRD) patterns of 4-aminosalicylic acid (4-ASA) and its derivatives are investigated in powder and thin film forms. Thermal properties of the compounds are investigated by thermogravemetric analysis (TGA). The optical energy gap and the type of optical transition are investigated in the wavelength range (200-2500 nm) for 4-ASA, HL and HLn. The values of fundamental energy gap (Eg) are in the range 3.60-3.69 eV for all compounds and the type of optical transition is found to be indirect allowed. The onset energy gap Eg∗ appeared only for azodye compounds is found to be in the range 0.95-1.55 eV depending on the substituent function groups. The refractive index, n, shows a normal dispersion in the wavelength range 650-2500 nm, while shows anomalous dispersion in the wavelength rang 200-650 nm. The dispersion parameters ε∞, εL, Ed, Eo and N /m∗ are calculated. The photoluminescence phenomena (PL) appear for thin films of 4-ASA and its derivatives show three main emission transitions.

  1. Characterization of pH-fractionated humic acids derived from Chinese weathered coal.

    Science.gov (United States)

    Zhang, Shuiqin; Yuan, Liang; Li, Wei; Lin, Zhian; Li, Yanting; Hu, Shuwen; Zhao, Bingqiang

    2017-01-01

    To reduce the compositional and structural heterogeneity of humic acids (HAs) and achieve better use of HA resources, in this study, we report a new sequential dissolution method for HAs derived from Chinese weathered coal. This method was used to separate HAs into seven fractions by adjusting the pH (3-10) of the extraction solution. The results showed that the HA fractions derived from Chinese weathered coal were concentrated up to 90.31% in the lower pH solutions (3-7). The compositional and structural characteristics of the HA fractions were determined by elemental analysis; ultraviolet-visible (UV-Vis), Fourier transform infrared (FTIR), and solid-state (13)C-nuclear magnetic resonance (NMR) spectroscopies; and other techniques. The results showed significant differences among the HA fractions. The concentrations of the total acidic groups and the carboxyl groups decreased with the increasing pH of the extraction solution. However, the HA fractions derived from extraction solutions with pH 3-4 had relatively lower aromaticity but a higher protonated carbon content. The HA fractions derived from extraction solutions with pH 6-7 had the highest aromaticity and the greatest abundance of COO/N-C=O. This study demonstrated that adjusting the pH of the extraction solution is one way to fractionate HAs from Chinese weathered coal and to obtain HA fractions with compositions and structures that could serve as useful material for study and utilization.

  2. Quantitative structure activity relationships of some pyridine derivatives as corrosion inhibitors of steel in acidic medium.

    Science.gov (United States)

    El Ashry, El Sayed H; El Nemr, Ahmed; Ragab, Safaa

    2012-03-01

    Quantum chemical calculations using the density functional theory (B3LYP/6-31G DFT) and semi-empirical AM1 methods were performed on ten pyridine derivatives used as corrosion inhibitors for mild steel in acidic medium to determine the relationship between molecular structure and their inhibition efficiencies. Quantum chemical parameters such as total negative charge (TNC) on the molecule, energy of highest occupied molecular orbital (E (HOMO)), energy of lowest unoccupied molecular orbital (E (LUMO)) and dipole moment (μ) as well as linear solvation energy terms, molecular volume (Vi) and dipolar-polarization (π) were correlated to corrosion inhibition efficiency of ten pyridine derivatives. A possible correlation between corrosion inhibition efficiencies and structural properties was searched to reduce the number of compounds to be selected for testing from a library of compounds. It was found that theoretical data support the experimental results. The results were used to predict the corrosion inhibition of 24 related pyridine derivatives.

  3. Characteristic of hyaluronic acid derivative films cross-linked by polyethylene glycol of low water content

    Institute of Scientific and Technical Information of China (English)

    Chen Jinghua; Chen Jingtao; Xu Zheng; Gu Qisheng

    2008-01-01

    Objective: To test the characteristics of byaluronic acid (HA) derivative cross-linked by polyethylene glycol films of low water content. Methods: The cross-linked HA film with 200 μm thickness was got at atmospheric pressure at 25℃ for 5 d. After dried, cross-linked films of 10 mm×10 mm were weighed and immersed in phosphate buffered saline (PBS pH 7.45) at 37℃ for 24 h. Then the solution fraction and water content were estimated. Meanwhile, cross-linked HA derivative films were immersed in phosphate buffered saline (PBS: pH 7.45) at 37℃ for determined time and then implanted subcutaneously in the back of white rats to test in vitro or in vivo degradation characteristic. Results and Conclusion: HA hydrogel cross-linked by polyethylene glycol with water content is as low as 60% and this kind of HA derivative has a slow degradation rate.

  4. The effect of short-chain fatty acids on human monocyte-derived dendritic cells

    DEFF Research Database (Denmark)

    Nastasi, Claudia; Candela, Marco; Bonefeld, Charlotte Menné

    2015-01-01

    negligible effects, while both butyrate and propionate strongly modulated gene expression in both immature and mature human monocyte-derived DC. An Ingenuity pathway analysis based on the differentially expressed genes suggested that propionate and butyrate modulate leukocyte trafficking, as SCFA strongly......The gut microbiota is essential for human health and plays an important role in the pathogenesis of several diseases. Short-chain fatty acids (SCFA), such as acetate, butyrate and propionate, are end-products of microbial fermentation of macronutrients that distribute systemically via the blood....... The aim of this study was to investigate the transcriptional response of immature and LPS-matured human monocyte-derived DC to SCFA. Our data revealed distinct effects exerted by each individual SCFA on gene expression in human monocyte-derived DC, especially in the mature ones. Acetate only exerted...

  5. Compound-specific isotopes of fatty acids as indicators of trophic interactions in the East China Sea ecosystem

    Science.gov (United States)

    Wu, Ying; Wang, Na; Zhang, Jing; Wan, Ruijing; Dai, Fangqun; Jin, Xianshi

    2016-09-01

    The composition and compound-specific isotopes of fatty acids were studied within food webs in the East China Sea. Lipid-normalized stable carbon isotopes of total organic carbon had a good correlation with trophic level. Variations in fatty acid compositions among diff erent species were observed but were unclear. Diff erent dietary structures could be traced from molecular isotopes of selected fatty acids in the Shiba shrimp ( Matapenaeus joyneri), the coastal mud shrimp ( Solenocera crassicornis) and the northern Maoxia shrimp ( Acetes chinensis). Both M. joyneri and S. crassicornis are mainly benthos feeders, while A. chinensis is a pelagic species, although they have a similar fatty acid composition. There was a good correlation for isotopes of arachidonic acid (C20:4n6; ARA) and docosahexaenoic acid (C22:6n3; DHA) among pelagic species from higher trophic levels. The isotopic compositions of DHA in benthic species were more negative than those of pelagic species at the same trophic level. The fact that the diet of benthic species contains more degraded items, the carbon isotopes of which are derived from a large biochemical fraction, may be the reason for this variation. A comparative study of benthic and pelagic species demonstrated the diff erent carbon sources in potential food items and the presence of a more complex system at the water-sediment interface.

  6. Selective Michael-type addition of a D-glucuronic acid derivative in the synthesis of model substances for uronic acid containing polysaccharides

    Directory of Open Access Journals (Sweden)

    2008-08-01

    Full Text Available A flexible protocol for the preparation of model substances for uronic acid containing polysaccharides is presented. We have synthesized a D-glucuronic acid derivative which is designed so that it easily can be conjugated with different structures and architectures by selective Michael-type addition. By successful coupling of the glucuronic acid derivative to polyethylene glycol with high degree of conversion, products were obtained that were easily characterized and which resembled polysaccharides in terms of solubility and purification methods that could be employed. The model substance can potentially be used to facilitate optimization of low-degree modification reactions of high molecular weight D-glucuronic acid containing polysaccharides.

  7. Photoluminescence of porous silicon as an indicator of its interaction with nucleic acids

    Science.gov (United States)

    Shevchenko, Victoriya B.; Dacenko, Oleksandr; Makara, Volodymyr; Golovynskyi, Sergii L.; Golovynska, Iuliia

    2017-01-01

    Changes in photoluminescence (PL) of porous silicon (PS), induced by treatment of its surface with nucleic acid solutions, were studied. It was found that such a treatment lead to an increase in PS PL intensity and shift of its peak to shorter wavelengths; the changes were shown to be dependent on the nucleic acid concentration in solution. Treatment with the solution of double-stranded DNA resulted in stronger change in PL than that caused by solution of single-stranded molecules of polynucleotide poly(A). Changes in the surface states of PS produced by the PS treatment with DNA solutions were investigated by means of infrared and electron paramagnetic resonance spectroscopy. The observed changes were explained by the PS oxidation. The presence of the nucleic acids in the aqueous solution significantly accelerates the PS oxidation process. A possible mechanism of the polynucleotide effect on the PS PL was discussed.

  8. Effect ofγ-aminobutyric acid combined with conventional aerosol inhalation therapy on serum indicators and induced sputum indicators of patients with asthma

    Institute of Scientific and Technical Information of China (English)

    Jun-Ning Li

    2016-01-01

    Objective:To analyze the effect ofγ-aminobutyric acid combined with conventional aerosol inhalation therapy on serum indicators and induced sputum indicators of patients with asthma. Methods:A total of 116 asthma patients receiving treatment in our hospital from July 2011 to August 2014 were included for study, and then all patients were divided into observation group (n=60) and control group (n=56). Differences in illness-related factor and protein expression in serum and induced sputum were compared between two groups.Results: Serum PDGF-BB, SP, LTE4 and CGRP levels of observation group after treatment were lower than those of control group, and TGFβ1 level was higher than that of control group (P<0.05); serum OPN, HSP70, Eotaxin and ECP expression levels of observation group after treatment were lower than those of control group, and VDBP and CC16 expression levels were higher than those of control group (P<0.05); SCF, M-CSF, CKLF1 and ICAM-1 levels in induced sputum of observation group after treatment were lower than those of control group (P<0.05); MCP-1, Gal-3, RAGE, HMGB1 and SDF-1 levels in induced sputum of observation group after treatment were lower than those of control group (P<0.05).Conclusions:After patients with asthma receivedγ-aminobutyric acid combined with conventional aerosol inhalation therapy, the levels of disease severity-related indicators in serum and induced sputum are optimized, and it has significant effect on disease treatment.

  9. Urolithins, ellagic acid-derived metabolites produced by human colonic microflora, exhibit estrogenic and antiestrogenic activities.

    Science.gov (United States)

    Larrosa, Mar; González-Sarrías, Antonio; García-Conesa, María Teresa; Tomás-Barberán, Francisco A; Espín, Juan Carlos

    2006-03-08

    Urolithins A and B (hydroxy-6H-dibenzo[b,d]pyran-6-one derivatives) are colonic microflora metabolites recently proposed as biomarkers of human exposure to dietary ellagic acid derivatives. Molecular models suggest that urolithins could display estrogenic and/or antiestrogenic activity. To this purpose, both urolithins and other known phytoestrogens (genistein, daidzein, resveratrol, and enterolactone) were assayed to evaluate the capacity to induce cell proliferation on the estrogen-sensitive human breast cancer MCF-7 cells as well as the ability to bind to alpha- and beta-estrogen receptors. Both urolithins A and B showed estrogenic activity in a dose-dependent manner even at high concentrations (40 microM), without antiproliferative or toxic effects, whereas the other phytoestrogens inhibited cell proliferation at high concentrations. Overall, urolithins showed weaker estrogenic activity than the other phytoestrogens. However, both urolithins displayed slightly higher antiestrogenic activity (antagonized the growth promotion effect of 17-beta-estradiol in a dose-dependent manner) than the other phytoestrogens. The IC(50) values for the ERalpha and ERbeta binding assays were 0.4 and 0.75 microM for urolithin A; 20 and 11 microM for urolithin B; 3 and 0.02 for genistein; and 2.3 and 1 for daidzein, respectively; no binding was detected for resveratrol and enterolactone. Urolithins A and B entered into MCF-7 cells and were metabolized to yield mainly urolithin-sulfate derivatives. These results, together with previous studies regarding absorption and metabolism of dietary ellagitannins and ellagic acid in humans, suggest that the gut microflora metabolites urolithins are potential endocrine-disrupting molecules, which could resemble other described "enterophytoestrogens" (microflora-derived metabolites with estrogenic/antiestrogenic activity). Further research is warranted to evaluate the possible role of ellagitannins and ellagic acid as dietary "pro-phytoestrogens".

  10. Radiation-sensitive indicator based on radiation-chemical formation of acids in polyvinyl butyral films containing chloral hydrate

    Science.gov (United States)

    Abdel-Fattah, Atef A.; El-Kelany, M.

    1998-03-01

    Radiation-sensitive indicators based on dyed polyvinyl butyral (PVB) containing acid-sensitive dye (bromophenol blue, BPB) and chloral hydrate (CCl 3CH(OH) 2, 2,2,2-trichloroethane-1, 1-diol) have been developed. These plastic film dosimeters undergo colour change from blue (the alkaline form of BPB) to yellow (the acidic form of BPB), indicating acid formation. The concentration of radiation-formed acids in the films containing different concentrations of chloral hydrate was calculated at different doses. The kinetics of the acid-formation reaction is discussed, indicating a half-order reaction with respect to chloral hydrate concentration. These films can be used as dosimeters for food irradiation applications where the maxima of the useful dose ranges are between 1 and 4 kGy depending on chloral hydrate concentration in the film. The response of these films depends on temperature during irradiation; therefore a correction should be applied. These films have the advantage of negligible humidity effects on response in the intermediate range of relative humidity from 10 to 70% as well as good post-irradiation stability when stored in the dark at room temperature.

  11. Comparative inhibitory effects of niflumic acid and novel synthetic derivatives on the rat isolated stomach fundus.

    Science.gov (United States)

    Criddle, David N; Meireles, AnaVanescaP; Macêdo, Liana B; Leal-Cardoso, José H; Scarparo, Henrique C; Jaffar, Mohammed

    2002-02-01

    Novel derivatives of 2-[3-(trifluoromethyl)-analino]nicotinic acid (niflumic acid) were synthesized. The compounds were compared for their inhibitory effects on 5-hydroxytryptamine (5-HT)- and KCI-induced contraction of the rat fundus. The aim was to assess structure-activity relationships regarding the selectivity and potency of these compounds. Niflumic acid (1-100 microM) concentration-dependently inhibited 5-HT-induced tonic contractions with an IC50 value (concentration reducing the control contractile response by 50%, calculated from semi-log graphs) of 0.24 x 10(4) M (n = 9). In contrast, it was significantly less potent at inhibiting KCl-induced responses (IC50 = 1.49 x 10(4) M, n = 9). The methyl ester (NFAme) and amido (NFAm) analogues showed no selectivity between 5-HT- and KCl-induced contractions with IC50 values of 1.64 x 10(-4) M (n = 8) and 1.87 x 10(-4) M (n = 9) for 5-HT responses, and 2.61 x 10(-4) M (n = 8) and 2.55 x 10(-4) M (n = 7) for KCl-induced responses, respectively. Our results suggest that alteration of the carboxylic acid moiety of niflumic acid reduces the selectivity and potency of its inhibitory action on 5-HT-induced contractile responses of the rat fundus, possibly via a reduced interaction with calcium-activated chloride channels.

  12. A novel acidic pH fluorescent probe based on a benzothiazole derivative.

    Science.gov (United States)

    Ma, Qiujuan; Li, Xian; Feng, Suxiang; Liang, Beibei; Zhou, Tiqiang; Xu, Min; Ma, Zhuoyi

    2017-04-15

    A novel acidic pH fluorescent probe 1 based on a benzothiazole derivative has been designed, synthesized and developed. The linear response range covers the acidic pH range from 3.44 to 6.46, which is valuable for pH researches in acidic environment. The evaluated pKa value of the probe 1 is 4.23. The fluorescence enhancement of the studied probe 1 with an increase in hydrogen ions concentration is based on the hindering of enhanced photo-induced electron transfer (PET) process. Moreover, the pH sensor possesses a highly selective response to H(+) in the presence of metal ions, anions and other bioactive small molecules which would be interfere with its fluorescent pH response. Furthermore, the probe 1 responds to acidic pH with short response time that was less than 1min. The probe 1 has been successfully applied to confocal fluorescence imaging in live HeLa cells and can selectively stain lysosomes. All of such good properties prove it can be used to monitoring pH fluctuations in acidic environment with high sensitivity, pH dependence and short response time.

  13. Production of chlorogenic acid and its derivatives in hairy root cultures of Stevia rebaudiana.

    Science.gov (United States)

    Fu, Xiao; Yin, Zhong-Ping; Chen, Ji-Guang; Shangguan, Xin-Chen; Wang, Xiaoqiang; Zhang, Qing-Feng; Peng, Da-Yong

    2015-01-14

    Chlorogenic acid and its derivatives (CADs) are valuable bioactive plant secondary metabolites with many health benefits. In the present study, Stevia rebaudiana hairy root cultures were established, and the culture conditions for the production of CADs were optimized. The hairy roots were induced by coculture of S. rebaudiana leaves and Agrobacterium rhizogenes (C58C1) after infection, which were further verified by PCR detection of rolB and rolC genes. HPLC-MS and HPLC analysis showed that chlorogenic acid (3-caffeoylquinic acid, 3-CQA), 3,5-dicaffeoylquinic acid (3,5-CQA), and 4,5-dicaffeoylquinic acid (4,5-CQA) were the major CADs in the hairy roots. Eight single roots with rapid growth rate were selected. Among them, T3 had the highest yield of CADs. B5 medium supplemented with 40 g/L sucrose was more suitable for the production of CADs than others. Under optimal culture conditions, the total content of these three compounds reached 105.58 mg/g and total yield was 234.40 mg/100 mL.

  14. [Antihypoxic effect of 3-hydroxypyridine and succinic acid derivatives and their nootropic action in alloxan diabetes].

    Science.gov (United States)

    Volchegorskiĭ, I A; Rassokhina, L M; Miroshnichenko, I Iu

    2011-01-01

    Relationship between the antihypoxic effect of 3-hydroxypyridine and succinic acid derivatives (emoxipine, reamberin and mexidol) and their effect on conditional learning, glycemia, and lipidemia was studied in rats with alloxan-induced diabetes. In parallel, the analogous relationship was investigated for alpha-lipoic acid that is regarded as a "gold standard" in treatment of diabetic neuropathy. It was established that single administration of emoxipine and mexidol in mice in doses equivalent to therapeutic-range doses in humans produces antihypoxic effect manifested by increased resistance to acute hypoxic hypoxia in test animals. Alpha-lipoic acid is inferior to emoxipin and mexidol in the degree of antihypoxic action. Reamberin does not exhibit this effect. The introduction of emoxipin, reamberin, mexidol, and alpha-lipoic acid in rats with alloxan diabetes during 7 or 14 days in doses equivalent to therapeutic-range doses in humans corrects conditional learning disorders in direct relationship with the antihypoxic activity of these drugs. The development of the nootropic effect of emoxipin, mexidol, and alpha-lipoic acid is related to a decrease in hyperglycemia and hyperlipidemia in rats with alloxan diabetes. The nootropic action of reamberin is accompanied by a transient hypoglycemizing effect and aggravation of dyslipidemic disorders. The antihypoxic activity of investigated drugs determines the direction and expression of their lipidemic effect, but is not correlated with the hypoglycemizing action these drugs on test animals with alloxan diabetes.

  15. Hydrolysis and rearrangement of phthalamic acid derivatives and assessment of their potential as prodrug forms for amines

    DEFF Research Database (Denmark)

    Bundgaard, H; Steffansen, B

    1990-01-01

    ] has claimed that N-(3-bromopropyl)phthalamic acid is very easily hydrolyzed in mildly alkaline solutions by an intramolecular catalytic effect of the ionized carboxy group. In this study, the degradation behaviour of N-(2-bromoethyl)phthalamic acid (I), N-(3-bromopropyl)phthalamic acid (II....... It is concluded that phthalamic acid derivatives are too stable chemically and enzymatically to be considered as prodrug forms for primary or secondary amines....

  16. Characteristics of Hyaluronic Acid Derivative Cross-linked by Polyethylene Glycol

    Institute of Scientific and Technical Information of China (English)

    2005-01-01

    Characteristic and dynamic viscosities of Hyaluronic acid ( HA ) derivative modified by polyethylene glycol (PEG) were tested with different reaction times (6 h,12 h,18 h and 24 h ) , different molar ratio of HA/PEG ( 1/10,1/5,1/3 and 1/2), different molecular weight of PEG(400,6 000 and 20 000) and mass fraction is 0.4% by Wushi Viscosimeter and L- 90 Rheometer at 25 ℃. Characteristic viscosity of HA derivative had the largest value in 12 h, which decreased with increasing of PEG molecular weight, but its aqueous dynamic viscosity increased with increment of PEG molecular weight. Meanwhile, we tested dynamic mechanic properties of HA derivative by 3ARES3 Rheometer at 25 ℃ to study viscoelastic changes and to compare change difference from viscosity to elasticity with the changes of vibration frequency between unmodified HA and HA derivative.Change from low vibrated frequency to high one of solution resulted in change from viscosity to elasticity of solution. In conclusion, as to the rheological properties, structure-modified HA derivative meets the requirement of biomnterial .

  17. Formation and Characterization of Self-Assembled Phenylboronic Acid Derivative Monolayers toward Developing Monosaccaride Sensing-Interface

    Directory of Open Access Journals (Sweden)

    Kwangnak Koh

    2007-08-01

    Full Text Available We designed and synthesized phenylboronic acid as a molecular recognitionmodel system for saccharide detection. The phenylboronic acid derivatives that haveboronic acid moiety are well known to interact with saccharides in aqueous solution; thus,they can be applied to a functional interface of saccharide sensing through the formation ofself-assembled monolayer (SAM. In this study, self-assembled phenylboronic acidderivative monolayers were formed on Au surface and carefully characterized by atomicforce microscopy (AFM, Fourier transform infrared reflection absorption spectroscopy(FTIR-RAS, surface enhanced Raman spectroscopy (SERS, and surface electrochemicalmeasurements. The saccharide sensing application was investigated using surface plasmonresonance (SPR spectroscopy. The phenylboronic acid monolayers showed goodsensitivity of monosaccharide sensing even at the low concentration range (1.0 × 10-12 M.The SPR angle shift derived from interaction between phenylboronic acid andmonosaccharide was increased with increasing the alkyl spacer length of synthesizedphenylboronic acid derivatives.

  18. Spectrophotometric determination of acidity constant of some indicators in various micellar media solutions by rank annihilation factor analysis.

    Science.gov (United States)

    Niazi, Ali; Zolgharnein, Javad; Davoodabadi, Mohammad Reza

    2008-07-01

    Rank annihilation factor analysis (RAFA) was used to the spectrophotometric studies of the acidity constant of methyl orange, methyl red and methyl violet in water and different micellar solutions at 25 degrees C and an ionic strength of 0.1M. When the acidity constants (surfactant concentration dependent acidity constant) acts as an optimizing object, and simply combined with the pure spectrum of acidic and basic forms, the rank of original data matrix can be reduced. The residual standard deviation (R.S.D.) of the residual matrix after bi-linearization of the background matrix is regarded as the evaluation function. Results show that the acidity constant of these indicators are influenced as the percentages of neutral, cationic and anionic surfactant such as Triton X-100 (poly(oxyethylene)(9.5)p-(1,1,3,3-tetramethyl), sodiumdodecylsulfate (SDS) and cethyltrimethylammonium (CTAB), respectively, added to the solution of these reagents. Also, RAFA is an efficient chemometrics algorithm for completely analysis of acid-base equilibrium systems by spectrophotometric method. Effects of surfactant on acidity constant and absorption spectra are also discussed.

  19. Multi-Component synthesis and computational studies of three novel thio-barbituric acid carbohydrate derivatives

    Science.gov (United States)

    Gupta, Stuti; Khare, Naveen K.

    2017-01-01

    The thio-barbituric acid is convenient starting compound for the preparation of fused heterocycles and its 5-substituted derivatives which are pharmacologically one of the most important classes of compounds. The fused compounds of thio-barbituric acid, 4-(1R,2S,3S,4S)-1,2,3,4,5-tetrahydroxy pentyl-10-phenyl-1,3,6,8,9,10 hexahydro-2,7-dithiooxopyrido [2,3-d; 6,5'] dipyrimidine-4,5 diones (1), 4-(1S,2S,3S,4S)-1,2,3,4,5-tetrahydroxy pentyl-10-phenyl-1,3,6,8,9,10 hexahydro-2,7-dithiooxopyrido [2,3-d; 6,5'] dipyrimidine-4,5 diones (2), 3-(1R,2S,3S)-1,2,3,4-tetrahydroxy butyl-10-phenyl-1,3,6,8,9,10 hexahydro-2,7-dithiooxopyrido [2,3-d; 6,5'] dipyrimidine-4,5 diones (3) have been synthesized in single step by the condensation of thio-barbituric acid with sugars (L-rhamnose, L-fucose and L-arabinose) & aniline using para-toluene sulfonic acid (p-TSA) as an effective acid catalyst under refluxing conditions. The molecular structure and detailed spectroscopic analysis of all three novel synthesized thiones derivatives have been performed using experimental techniques like 1H, 13C NMR, 2D (COSY, HSQC, DEPT-135 and DEPT-90) as well as theoretical calculations by density functional theory (DFT) using B3LYP and 6-311G + (d, p) basis set. The strength and nature of weak intramolecular interactions have been studied by atom in molecule (AIM) approach. Global reactivity descriptors have been computed to predict reactivity and reactive sites in the molecule.

  20. Colour indicator for enantiomeric excess and assignment of the configuration of the major enantiomer of an amino acid ester

    NARCIS (Netherlands)

    Delden, R.A.van; Feringa, B.L.

    2002-01-01

    A colour indicator for the full range of enantiomeric excess (-100% --> 100% ee) is presented which is based on visual colour inspection of a liquid crystal doped with the analyte, i.e. the methyl ester of amino acid phenylglycine, providing the enantiomeric excess and allowing the assignment of the

  1. Generation and dietary modulation of anti-inflammatory electrophilic omega-3 fatty acid derivatives.

    Directory of Open Access Journals (Sweden)

    Chiara Cipollina

    Full Text Available Dietary ω-3 polyunsaturated fatty acids (PUFAs decrease cardiovascular risk via suppression of inflammation. The generation of electrophilic α,β-unsaturated ketone derivatives of the ω-3 PUFAs docosahexaenoic acid (DHA and docosapentaenoic acid (DPA in activated human macrophages is catalyzed by cyclooxygenase-2 (Cox-2. These derivatives are potent pleiotropic anti-inflammatory signaling mediators that act via mechanisms including the activation of Nrf2-dependent phase 2 gene expression and suppression of pro-inflammatory NF-κB-driven gene expression. Herein, the endogenous generation of ω-3 PUFAs electrophilic ketone derivatives and their hydroxy precursors was evaluated in human neutrophils. In addition, their dietary modulation was assessed through a randomized clinical trial.Endogenous generation of electrophilic omega-3 PUFAs and their hydroxy precursors was evaluated by mass spectrometry in neutrophils isolated from healthy subjects, both at baseline and upon stimulation with calcium ionophore. For the clinical trial, participants were healthy adults 30-55 years of age with a reported EPA+DHA consumption of ≤300 mg/day randomly assigned to parallel groups receiving daily oil capsule supplements for a period of 4 months containing either 1.4 g of EPA+DHA (active condition, n = 24 or identical appearing soybean oil (control condition, n = 21. Participants and laboratory technicians remained blinded to treatment assignments.5-lypoxygenase-dependent endogenous generation of 7-oxo-DHA, 7-oxo-DPA and 5-oxo-EPA and their hydroxy precursors is reported in human neutrophils stimulated with calcium ionophore and phorbol 12-myristate 13-acetate (PMA. Dietary EPA+DHA supplementation significantly increased the formation of 7-oxo-DHA and 5-oxo-EPA, with no significant modulation of arachidonic acid (AA metabolite levels.The endogenous detection of these electrophilic ω-3 fatty acid ketone derivatives supports the precept that the

  2. A PRELIMINARY INVESTIGATION INTO THE USE OF ACID-TOLERANT PRECIPITATED CALCIUM CARBONATE FILLERS IN PAPERMAKING OF DEINKED PULP DERIVED FROM RECYCLED NEWSPAPER

    Directory of Open Access Journals (Sweden)

    Jing Shen

    2009-08-01

    Full Text Available The use of acid-tolerant precipitated calcium carbonate fillers, including phosphoric acid/sodium hexametaphosphate modified precipitated CaCO3 filler, and sodium silicate/phosphoric acid/sodium hexametaphos-phate modified precipitated CaCO3 filler in papermaking of deinked pulp derived from recycled newspaper was explored. These two acid-tolerant fillers provided considerably more brightness improvement in papers in comparison the unmodified filler, presumably indicating alleviated pulp darkening achieved as a result of better acid-resistant properties. The addition of acid-tolerant fillers into the furnish slurries gave lower system pH as compared with unmodified filler. Among the three fillers used in this work, the effect on retention of modification of the filler with sodium silicate/phosphoric acid/sodium hexametaphosphate was probably the best, as evaluated from ash content measurements. For air permeability of the paper, the use of acid-tolerant fillers provided slightly more improvement in comparison to the unmodified filler. For tensile and burst strength of the paper, the use of sodium silicate/phosphoric acid/sodium hexameta-phosphate modified precipitated calcium carbonate filler gave better results as compared with the other two fillers. Additionally, the improving effect of acid-tolerant fillers on furnish static drainage was found to be slightly weaker than that of unmodified filler.

  3. Relative and absolute reliability of measures of linoleic acid-derived oxylipins in human plasma.

    Science.gov (United States)

    Gouveia-Figueira, Sandra; Bosson, Jenny A; Unosson, Jon; Behndig, Annelie F; Nording, Malin L; Fowler, Christopher J

    2015-09-01

    Modern analytical techniques allow for the measurement of oxylipins derived from linoleic acid in biological samples. Most validatory work has concerned extraction techniques, repeated analysis of aliquots from the same biological sample, and the influence of external factors such as diet and heparin treatment upon their levels, whereas less is known about the relative and absolute reliability of measurements undertaken on different days. A cohort of nineteen healthy males were used, where samples were taken at the same time of day on two occasions, at least 7 days apart. Relative reliability was assessed using Lin's concordance correlation coefficients (CCC) and intraclass correlation coefficients (ICC). Absolute reliability was assessed by Bland-Altman analyses. Nine linoleic acid oxylipins were investigated. ICC and CCC values ranged from acceptable (0.56 [13-HODE]) to poor (near zero [9(10)- and 12(13)-EpOME]). Bland-Altman limits of agreement were in general quite wide, ranging from ±0.5 (12,13-DiHOME) to ±2 (9(10)-EpOME; log10 scale). It is concluded that relative reliability of linoleic acid-derived oxylipins varies between lipids with compounds such as the HODEs showing better relative reliability than compounds such as the EpOMEs. These differences should be kept in mind when designing and interpreting experiments correlating plasma levels of these lipids with factors such as age, body mass index, rating scales etc.

  4. High-throughput lipidomic analysis of fatty acid derived eicosanoids and N-acylethanolamines.

    Science.gov (United States)

    Dumlao, Darren S; Buczynski, Matthew W; Norris, Paul C; Harkewicz, Richard; Dennis, Edward A

    2011-11-01

    Fatty acid-derived eicosanoids and N-acylethanolamines (NAE) are important bioactive lipid mediators involved in numerous biological processes including cell signaling and disease progression. To facilitate research on these lipid mediators, we have developed a targeted high-throughput mass spectrometric based methodology to monitor and quantitate both eicosanoids and NAEs, and can be analyzed separately or together in series. Each methodology utilizes scheduled multiple reaction monitoring (sMRM) pairs in conjunction with a 25 min reverse-phase HPLC separation. The eicosanoid methodology monitors 141 unique metabolites and quantitative amounts can be determined for over 100 of these metabolites against standards. The analysis covers eicosanoids generated from cycloxygenase, lipoxygenase, cytochrome P450 enzymes, and those generated from non-enzymatic pathways. The NAE analysis monitors 36 metabolites and quantitative amounts can be determined for 33 of these metabolites against standards. The NAE method contains metabolites derived from saturated fatty acids, unsaturated fatty acids, and eicosanoids. The lower limit of detection for eicosanoids ranges from 0.1pg to 1pg, while NAEs ranges from 0.1pg to 1000pg. The rationale and design of the methodology is discussed.

  5. Catalytic Kinetic Determination of Micro Amounts of Oxalic Acid by Second-Order Derivative Oscillopolarography

    Institute of Scientific and Technical Information of China (English)

    2001-01-01

    It was found that micro amounts of oxalate showed a very strong catalytic effect on the slow reaction between K2Cr2O7 and Orange Ⅳ in a diluted sulfuric acid medium in a water bath at 70 ℃. Orange Ⅳ exhibited a sensitive second-order derivative polarographic wave at -0.50 V(vs. SCE). This provides the basis for a sensitive and selective catalytic kinetic method for oxalate determination with second-order derivative oscillopolarography. The effects of sulphuric acid, K2Cr2O7, and orange Ⅳ concentrations, reaction temperature and reaction time were investigated. A calibration curve of oxalate in the range of 0.1—2.0 μg/mL was obtained by the fixed-time procedure. The detection limit was 0.03 μg/ mL. The possible interference from co-existing substances or ions was examined. The new method has a high sensitivity and a good selectivity compared to other existing methods for oxalic acid determination. It has been applied to the determination of micro amounts of oxalate in real urine samples with satisfactory results.

  6. Production of fatty acid-derived oleochemicals and biofuels by synthetic yeast cell factories.

    Science.gov (United States)

    Zhou, Yongjin J; Buijs, Nicolaas A; Zhu, Zhiwei; Qin, Jiufu; Siewers, Verena; Nielsen, Jens

    2016-01-01

    Sustainable production of oleochemicals requires establishment of cell factory platform strains. The yeast Saccharomyces cerevisiae is an attractive cell factory as new strains can be rapidly implemented into existing infrastructures such as bioethanol production plants. Here we show high-level production of free fatty acids (FFAs) in a yeast cell factory, and the production of alkanes and fatty alcohols from its descendants. The engineered strain produces up to 10.4 g l(-1) of FFAs, which is the highest reported titre to date. Furthermore, through screening of specific pathway enzymes, endogenous alcohol dehydrogenases and aldehyde reductases, we reconstruct efficient pathways for conversion of fatty acids to alkanes (0.8 mg l(-1)) and fatty alcohols (1.5 g l(-1)), to our knowledge the highest titres reported in S. cerevisiae. This should facilitate the construction of yeast cell factories for production of fatty acids derived products and even aldehyde-derived chemicals of high value.

  7. Inhibitory effects of gallic acid ester derivatives on Saccharomyces cerevisiae multidrug resistance protein Pdr5p.

    Science.gov (United States)

    Pereira Rangel, Luciana; Fritzen, Márcio; Yunes, Rosendo Augusto; Leal, Paulo César; Creczynski-Pasa, Tânia Beatriz; Ferreira-Pereira, Antônio

    2010-05-01

    Overexpression of the Saccharomyces cerevisiae ABC transporter Pdr5p confers resistance to a range of structurally unrelated xenobiotics. This property allows Pdr5p to be used as a target for novel multidrug resistance reversal reagents or chemosensitizers. Herein, we report the effects of gallic acid derivatives with substitutions either on the ester moiety or in the benzene ring on the activity of Pdr5p. Compounds with a longer side chain (8-16 carbons) resulted in greater inhibition of Pdr5p ATPase. Derivatives with side chains of 8-12 carbons that retained hydroxyl groups on the benzene ring extensively inhibited Pdr5p ATPase activity. These compounds almost completely inhibited the efflux of the Pdr5p fluorescent substrate Rhodamine 6G and at 25 muM chemosensitized the Pdr5p-overexpressing strain AD124567 to fluconazole (0.4 mg mL(-1)). Gallic acid derivatives may be a new class of Pdr5p inhibitors.

  8. Enantioselective separation of amino acids as biomarkers indicating life in extraterrestrial environments.

    Science.gov (United States)

    Pietrogrande, Maria Chiara

    2013-10-01

    Traces of prebiotic amino acids, i.e., the building blocks of proteins, are excellent biomarkers that could provide evidence of extinct or extant life in extra-terrestrial environments. In particular, characterization of the enantiomeric excess of amino acids gives relevant information about the biotic or abiotic origin of molecules, because it is generally assumed that life elsewhere could be based on either L or D amino acids, but not both. The analytical procedures used in in-situ space missions for chiral discrimination of amino acids must meet severe requirements imposed by flight conditions: short analysis time, low energy consumption, robustness, storage for long periods under extreme conditions, high efficiency and sensitivity, automation, and remote-control operation. Such methods are based on gas chromatography, high-pressure liquid chromatography, and capillary electrophoresis, usually coupled with mass spectrometry; of these, gas chromatography-mass spectrometry (GC-MS) is the only such combination yet used in space missions. Preliminary in-situ sample derivatization is required before GC-MS analysis to convert amino acids into volatile and thermally stable compounds. The silylation reagent most commonly used, N-(tert-butyldimethylsilyl)-N-methyltrifluoroacetamide, is unsuitable for detection of homochirality, and alternative derivatization techniques have been developed that preserve the stereochemical configuration of the original compounds and are compatible with spaceflight conditions. These include the reagent N,N-dimethylformamide dimethylacetal, which has already been used in the Rosetta mission, a mixture of alkyl chloroformate, ethanol, and pyridine, a mixture of perfluorinated anhydrides and perfluoro alcohols, and hexafluoroacetone, the first gaseous derivatizing agent. In all the space instruments, solvent extraction of organic matter and chemical derivatization have been combined in a single automatic and remote-controlled procedure in a

  9. Plasma acylcarnitine profiling indicates increased fatty acid oxidation relative to tricarboxylic acid cycle capacity in young, healthy low birth weight men

    DEFF Research Database (Denmark)

    Ribel-Madsen, Amalie; Ribel-Madsen, Rasmus; Brøns, Charlotte;

    2016-01-01

    measured fasting plasma levels of 45 acylcarnitine species in 18 LBW and 25 NBW men after an isocaloric control diet and a 5‐day high‐fat, high‐calorie diet. We demonstrated that LBW men had higher C2 and C4‐OH levels after the control diet compared with NBW men, indicating an increased fatty acid beta...

  10. Application of acetate derivatives for gas chromatography-mass spectrometry: novel approaches on carbohydrates, lipids and amino acids analysis.

    Science.gov (United States)

    Sassaki, Guilherme L; Souza, Lauro M; Serrato, Rodrigo V; Cipriani, Thales R; Gorin, Philip A J; Iacomini, Marcello

    2008-10-24

    The structure of glycoconjugates has been determined by several chromatographic methods, however gas chromatography-mass spectrometry (GC-MS) has been widely used to identify and quantify the volatile trimethylsilyl and fluoroacyl derivatives. Adapting the reduction/acetylation strategies, we had performed the derivatization of all monosaccharide class, as well as amino acids and OH-fatty acids as from different glycoconjugates. Uronic acids gave characteristic ions at m/z 143, 156 and 173, and 19 amino acids derivatives, gave molecular ions [M]+ and daughter ions of [M-59]+ and [M-43]+ on electron impact (EI)-MS, which provide their rapid identification.

  11. The effect of trinitrobenzene sulfonic acid on gut-derived smooth muscle cell arachidonic acid metabolism: role of endogenous prostanoids

    Directory of Open Access Journals (Sweden)

    W. E. Longo

    1997-01-01

    Full Text Available The contribution of smooth muscle cells as a potential source of eicosanoid production during inflammatory states remains to be elucidated. We investigated the effect of trinitrobenzene sulfonic acid (TNB, a known pro-inflammatory agent, on jejunal smooth muscle cell eicosanoid production. Human gut-derived smooth muscle cells (HISM were incubated with TNB for 1 hour. Additionally, some cells were preincubated with either dimethylthiourea, or indomethacin for 1 hour before exposure to identical concentrations of TNB. Incubation with TNB led to significant increases in PGE2 and 6-keto PGF-1α release, but not leukotriene B4 release; responses which were both inhibited by dimethylthiourea and indomethacin treatment. Our results suggest that gutderived smooth muscle cells may represent an important source of proinflammatory prostanoids but not leukotrienes during inflammatory states of the intestine. The inhibition of prostanoid activity by thiourea may be mediated by suppression of cyclooxygenase activity in this cell line.

  12. Root-uptake of {sup 14}C derived from acetic acid and {sup 14}C transfer to rice edible parts

    Energy Technology Data Exchange (ETDEWEB)

    Ogiyama, Shinichi [Office of Biospheric Assessment for Waste Disposal, National Institute of Radiological Sciences, 4-9-1 Anagawa, Inage-ku, Chiba-shi 263-8555 (Japan)], E-mail: ogiyama@nirs.go.jp; Suzuki, Hiroyuki [Graduate School of Pharmaceutical Sciences, Chiba University, 1-33 Yayoi-cho, Inage-ku, Chiba-shi 263-5522 (Japan); Inubushi, Kazuyuki [Graduate School of Horticulture, Chiba University, 648 Matsudo, Matsudo-shi 271-8510 (Japan); Takeda, Hiroshi; Uchida, Shigeo [Office of Biospheric Assessment for Waste Disposal, National Institute of Radiological Sciences, 4-9-1 Anagawa, Inage-ku, Chiba-shi 263-8555 (Japan)

    2010-02-15

    Three types of culture experiments using paddy rice (Oryza sativa L.) were performed to examine root-uptake of {sup 14}C in the form of acetic acid: double pot experiment (hydroponics), wet culture experiment (submerged sand medium), and chamber experiment (hydroponics and submerged sand medium). The {sup 14}C radioactivity in the plant, mediums, and atmospheric carbon dioxide ({sup 14}CO{sub 2}) in the chamber were determined, and the distribution of {sup 14}C in the plant was visualized using autoradiography. In the double pot experiment, the shoot of the plant and the lower root which was soaked in the culture solution had {sup 14}C radioactivity, but the upper root which did not have contact with the solution had none. There were also {sup 14}C radioactivity in the grains and roots in the wet culture experiment. Results of the chamber experiment showed that {sup 14}CO{sub 2} gas was released from the culture solution in both types of cultures. Results indicated that the {sup 14}C-acetic acid absorbed by rice plant through its root would be very small. Most of the {sup 14}C-acetic acid was transformed into gaseous forms either in the culture solution or rhizosphere. A relatively longer time would be needed to assimilate {sup 14}C derived from acetic acid to grain parts after it was once absorbed by the shoot through the root. Availability of {sup 14}C for the plant in sand culture was considered to be decreased compared with that for the plant in the hydroponics experiment. It was suggested that rice plant absorbed and assimilated {sup 14}C through the plant roots not because of uptake of {sup 14}C-acetic acid but because of uptake of {sup 14}C in gaseous forms such as {sup 14}CO{sub 2}.

  13. Involvement of dynamin-related protein 1 in free fatty acid-induced INS-1-derived cell apoptosis.

    Science.gov (United States)

    Peng, Liang; Men, Xiuli; Zhang, Wenjian; Wang, Haiyan; Xu, Shiqing; Fang, Qing; Liu, Honglin; Yang, Wenying; Lou, Jinning

    2012-01-01

    Elevated extracellular free fatty acids (FFAs) can induce pancreatic beta cell apoptosis, thereby contributing to the pathogenesis of type 2 diabetes mellitus (T2D). Mitochondrial dysfunction has been implicated in FFA-induced beta cell apoptosis. However, molecular mechanisms linking mitochondrial dysfunction and FFA-induced beta cell apoptosis are not clear. Dynamin-related protein 1 (DRP-1) is a mitochondrial fission modulator. In this study, we investigated its role in FFA-induced INS-1 beta cell apoptosis. DRP-1 protein was promptly induced in INS-1 cells and rat islets after stimulation by FFAs, and this DRP-1 upregulation was accompanied by increased INS-1 cell apoptosis. Induction of DRP-1 expression significantly promoted FFA-induced apoptosis in DRP-1 WT (DRP-1 wild type) inducible INS-1-derived cell line, but not in DRP-1K38A (a dominant negative mutant of DRP-1) inducible INS-1-derived cell line. To validate these in vitro results, we transplanted DRP-1 WT or DRP-1 K38A cells into renal capsules of streptozotocin (STZ)-treated diabetic mice to study the apoptosis in xenografts. Consistent with the in vitro results, the over-expression of DRP-1 led to aggravated INS-1-derived cell apoptosis triggered by FFAs. In contrast, dominant-negative suppression of DRP-1 function as represented by DRP-1 K38A significantly prevented FFA-induced apoptosis in xenografts. It was further demonstrated that mitochondrial membrane potential decreased, while cytochrome c release, caspase-3 activation, and generation of reactive oxygen species (ROS) were enhanced by the induction of DRP-1WT, but prevented by DRP-1 K38A in INS-1-derived cells under FFA stimulation. These results indicated that DRP-1 mediates FFA-induced INS-1-derived cell apoptosis, suggesting that suppression of DRP-1 is a potentially useful therapeutic strategy for protecting against beta cell loss that leads to type 2 diabetes.

  14. Cross-Sectional Associations between Empirically-Derived Dietary Patterns and Indicators of Disease Risk among University Students

    Directory of Open Access Journals (Sweden)

    Stacy A. Blondin

    2015-12-01

    Full Text Available The transition from adolescence to adulthood is a unique period during which lifelong dietary habits are shaped. Dietary patterns (DPs among young adults attending college have not been adequately described, and associations between DPs and indicators of disease risk are not well understood in this age group. Dietary data were collected from undergraduates participating in the Tufts Longitudinal Health Study (TLHS; 1998–2007 by Food Frequency Questionnaire (FFQ; n = 1323. DPs were derived using principal components analysis with varimax rotation. Scree plots; eigenvalues; factor loadings; and previous studies were used to determine and label the DPs retained. Cross-sectional relationships between DP scores and anthropometric measures (percent body fat (PBF and (BMI and lipid biomarkers (total; HDL and LDL cholesterol; and triglycerides were assessed with multivariable regression models; adjusted for demographics; physical activity; smoking; intention to gain/lose weight; and total energy intake. Effect modification by sex was tested. Three DPs were identified: Prudent; Western; and Alcohol. Greater adherence to the Prudent DP was associated with favorable anthropometric outcomes. The Alcohol DP was associated with a favorable lipid profile. Associations between the Western DP and blood lipids differed by sex; with unfavorable impact observed only among males. Our findings add to the literature linking DPs in young adults with measurable adiposity and cardiometabolic outcomes; suggesting that improving nutrition among college students could reduce chronic disease risk.

  15. Cross-Sectional Associations between Empirically-Derived Dietary Patterns and Indicators of Disease Risk among University Students

    Science.gov (United States)

    Blondin, Stacy A.; Mueller, Megan P.; Bakun, Peter J.; Choumenkovitch, Silvina F.; Tucker, Katherine L.; Economos, Christina D.

    2015-01-01

    The transition from adolescence to adulthood is a unique period during which lifelong dietary habits are shaped. Dietary patterns (DPs) among young adults attending college have not been adequately described, and associations between DPs and indicators of disease risk are not well understood in this age group. Dietary data were collected from undergraduates participating in the Tufts Longitudinal Health Study (TLHS; 1998–2007) by Food Frequency Questionnaire (FFQ; n = 1323). DPs were derived using principal components analysis with varimax rotation. Scree plots; eigenvalues; factor loadings; and previous studies were used to determine and label the DPs retained. Cross-sectional relationships between DP scores and anthropometric measures (percent body fat (PBF) and (BMI) and lipid biomarkers (total; HDL and LDL cholesterol; and triglycerides) were assessed with multivariable regression models; adjusted for demographics; physical activity; smoking; intention to gain/lose weight; and total energy intake. Effect modification by sex was tested. Three DPs were identified: Prudent; Western; and Alcohol. Greater adherence to the Prudent DP was associated with favorable anthropometric outcomes. The Alcohol DP was associated with a favorable lipid profile. Associations between the Western DP and blood lipids differed by sex; with unfavorable impact observed only among males. Our findings add to the literature linking DPs in young adults with measurable adiposity and cardiometabolic outcomes; suggesting that improving nutrition among college students could reduce chronic disease risk. PMID:26712784

  16. Salt-inducible promoter derivable from a lactic acid bacterium, and its use in a lactic acid bacterium for production of a desired protein

    NARCIS (Netherlands)

    Sanders, Jan Willem; Kok, Jan; Venema, Gerard; Ledeboer, Adrianus Marinus

    1998-01-01

    The invention provides a salt-inducible promoter present in SEQ ID NO: 10 and derivable from a lactic acid bacterium in isolation from the coding sequence normally controlled by said promoter in a wild-type lactic acid bacterium, with modifications and important parts thereof. Also provided are a re

  17. Theoretical Studies on Electronic Spectra and Second-order Nonlinear Optical Properties of Barbituric Acid Derivatives Substituted with Schiff Base

    Institute of Scientific and Technical Information of China (English)

    SUN,Gang(孙刚); QIU,Yong-Qing(仇永清); SUN,Hai-Zhu(孙海珠); SU,Zhong-Min(苏忠民); FENG,Jing-Dong(冯静东); ZHU,Yu-Lan(朱玉兰)

    2004-01-01

    The structures of barbituric acid derivatives substituted with Schiff base were optimized using ab initio HF method at 6-31G basis set.Based on the optimized structures,the electronic spectra were obtained by INDO/CI method.The second-order nonlinear optical (NLO) coefficients βu were calculated according to the sum-over-states (SOS) formula.In addition,the effect of conjugation on electronic spectra and second-order NLO coefficients was investigated.The influence of exchange between C and N atoms as well as the substituted effect on the barbituric acid was discussed.It was indicated that the exchange between C and N atoms on Schiff base is important for enhancing the NLO coefficient of the whole molecule with donor and acceptor (D-A).Meanwhile significant changes in electron donation and acception were observed as substituents changes positions.Among the designed models,molecule 1b has maximal βμ value of 124.65 × 10-30 esu.About molecule 1b,barbituric acid is considered as an accepted electronic group and the position of N atom on Schiff base is close to it.

  18. Synthesis of Eu(Ⅲ) and Tb(Ⅲ) complexes with novel pyridine dicarboxylic acid derivatives and their fluorescence properties

    Institute of Scientific and Technical Information of China (English)

    Tang Ruiren; Yan Zi'er; Guo Cancheng; Luo Yiming

    2006-01-01

    Starting from pyridine-2,6-dicarboxylic acid (DPA),a series of novel pyridine-2,6-dicarboxylic acid derivatives were synthesized.In these compounds,4-(hydroxymethyl)pyridine-2,6-dicarboxylate (4-HMDPA) and 4-[(bis-carboxymethyl-amino)-methyl] -pyridine-2,6-dicarboxylic acid (4-BMDPA) were used as multifunctional ligands to coordinate with Tb(Ⅲ) and Eu(Ⅲ) and the complexes were prepared.The fluorescence properties of the solid complexes and their solutions were investigated in detail.The results indicated that the weak election-withdrawing group 4-hydroxymethyl in 4-position of pyridine in 4-HMDPA could weaken the fluorescence intensity of the lanthanide complexes.The contradistinctive experimental results showed that the fluorescence intensities of these complexes are related to pH values of the aqueous solutions and the dipole moments of solvent molecules:in the neutral aqueous solutions,the fluorescence intensities of these complexes were strongest,while the dipole moments were lower when the fluorescence intensifies were stronger.4-BMDPA is the better sensitizer and may be used as time-resolved fluoroimmunoassay.

  19. Synthesis and anticancer evaluation of 2-phenyl thiaolidinone substituted 2-phenyl benzothiazole-6-carboxylic acid derivatives

    Directory of Open Access Journals (Sweden)

    Padmavathi P. Prabhu

    2015-03-01

    Full Text Available A novel series of 2-(3-(4-oxo-2-substituted phenyl thiazolidin-3-ylphenylbenzo[d]thiazole-6-carboxylic acid derivatives PP1–PP8 were synthesized by various benzothiazole Schiff’s bases by reaction with thioglycollic acid. Their structures were established on the basis of IR, 1H-NMR, 13C-NMR, mass spectral data and elemental analysis. All the synthesized compounds were screened for their in vitro anticancer activity by 3-(4,5-dimethyl thiazole-2yl-2,5-diphenyltetrazoliumbromide (MTT assay on human cervical cancer cell line (HeLa cell lines. Among these compound PP2 exhibited most significant activity as compared with PP5, PP7 and PP8. However, the activity was less as compared to the standard drug Cisplatin.

  20. Synthesis and Structural Characterization of 1- and 2-Substituted Indazoles: Ester and Carboxylic Acid Derivatives

    Directory of Open Access Journals (Sweden)

    Isabel Bento

    2006-11-01

    Full Text Available A series of indazoles substituted at the N-1 and N-2 positions with ester-containing side chains -(CH2nCO2R of different lengths (n = 0-6, 9, 10 are described.Nucleophilic substitution reactions on halo esters (X(CH2nCO2R by 1H-indazole inalkaline solution lead to mixtures of N-1 and N-2 isomers, in which the N-1 isomerpredominates. Basic hydrolysis of the ester derivatives allowed the synthesis of thecorresponding indazole carboxylic acids. All compounds were fully characterised bymultinuclear NMR and IR spectroscopies, MS spectrometry and elemental analysis; theNMR spectroscopic data were used for structural assignment of the N-1 and N-2 isomers.The molecular structure of indazol-2-yl-acetic acid (5b was determined by X-raydiffraction, which shows a supramolecular architecture involving O2-H...N1intermolecular hydrogen bonds.

  1. N-( p-Ethynylbenzoyl) derivatives of amino acid and dipeptide methyl esters - Synthesis and structural study

    Science.gov (United States)

    Eißmann, Frank; Weber, Edwin

    2011-11-01

    A series of N-( p-ethynylbenzoyl) derivatives ( 1-4) of the amino acids glycine and L-alanine as well as the dipeptides glycylglycine and L-alanylglycine has been synthesized via a two-step reaction sequence including the reaction of an appropriate N-( p-bromobenzoyl) precursor with trimethylsilylacetylene followed by deprotection of the trimethylsilyl protecting group, respectively. X-ray crystal structures of the amino acid and dipeptide methyl esters 1-4 are reported. The amide and peptide bonds within each molecular structure are planar and adopt the trans-configuration. The packing structures are governed by N sbnd H⋯O interactions leading to the formation of characteristic strand motifs. Further stabilization results from weaker C sbnd H⋯O and C sbnd H⋯π contacts.

  2. Design, synthesis and antitumor activity of novel D-glucuronic acid derivatives.

    Science.gov (United States)

    el-Nezhawy, Ahmed O H; Adly, Frady G; Eweas, Ahmed F; Hanna, Atef G; el-Kholy, Yehya M; el-Syed, Shahenaz H; el-Naggar, Tarek B A

    2011-11-01

    A series of D-glucuronic acid derivatives were chemically synthesized including acetylated and deacetylated glucuronamides, as well as N-glucuronides starting from the D-glucuronic acid itself by means of protection/deprotection, activation and condensation protocols. Structure elucidation of all products along with optimization of the synthetic steps is described. The synthesized compounds were evaluated for their in vitro antitumor activity against MCF-7, TK-10 and UACC-62 cell lines. The compounds 4, 5, 7, 8, 14, 16 and 18 were the most active against TK-10 cell line. On the other hand, the most active compounds against the MCF-7 cell line were 9, 18 and 20. However, compounds 7-10 13-15 and 17 were the most active against the UACC-62 cell line.

  3. Linoleic acid derivative DCP-LA improves learning impairment in SAMP8.

    Science.gov (United States)

    Yaguchi, Takahiro; Nagata, Tetsu; Mukasa, Takeshi; Fujikawa, Hirokazu; Yamamoto, Hideyuki; Yamamoto, Satoshi; Iso, Hiroyuki; Tanaka, Akito; Nishizaki, Tomoyuki

    2006-01-23

    In the water-maze test, the linoleic acid derivative, 8-[2-(2-pentyl-cyclopropylmethyl)-cyclopropyl]-octanoic acid (DCP-LA) (1 mg/kg, intraperitoneally), significantly shortened the prolonged latency for accelerated-senescence-prone mice 8 (SAMP8), reaching a level similar to the latency for accelerated-senescence-resistant mice 1 (SAMR1) as control. In the open-field test to assess motor activity, it was confirmed that the DCP-LA effect is not due to increased motor activity. In the passive avoidance test to assess fear memory, DCP-LA had no effect on the latency of acquisition and retention for SAMP8. The results of the present study, thus, suggest that DCP-LA could improve age-related learning impairment by enhancing cognitive functions.

  4. Diverse Bacterial PKS Sequences Derived From Okadaic Acid-Producing Dinoflagellates

    Directory of Open Access Journals (Sweden)

    Kathleen S. Rein

    2008-05-01

    Full Text Available Okadaic acid (OA and the related dinophysistoxins are isolated from dinoflagellates of the genus Prorocentrum and Dinophysis. Bacteria of the Roseobacter group have been associated with okadaic acid producing dinoflagellates and have been previously implicated in OA production. Analysis of 16S rRNA libraries reveals that Roseobacter are the most abundant bacteria associated with OA producing dinoflagellates of the genus Prorocentrum and are not found in association with non-toxic dinoflagellates. While some polyketide synthase (PKS genes form a highly supported Prorocentrum clade, most appear to be bacterial, but unrelated to Roseobacter or Alpha-Proteobacterial PKSs or those derived from other Alveolates Karenia brevis or Crytosporidium parvum.

  5. Arachidonic Acid Derivatives and Their Role in Peripheral Nerve Degeneration and Regeneration

    Directory of Open Access Journals (Sweden)

    Carlos Rodrigo Camara-Lemarroy

    2012-01-01

    Full Text Available After peripheral nerve injury, a process of axonal degradation, debris clearance, and subsequent regeneration is initiated by complex local signaling, called Wallerian degeneration (WD. This process is in part mediated by neuroglia as well as infiltrating inflammatory cells and regulated by inflammatory mediators such as cytokines, chemokines, and the activation of transcription factors also related to the inflammatory response. Part of this neuroimmune signaling is mediated by the innate immune system, including arachidonic acid (AA derivatives such as prostaglandins and leukotrienes. The enzymes responsible for their production, cyclooxygenases and lipooxygenases, also participate in nerve degeneration and regeneration. The interactions between signals for nerve regeneration and neuroinflammation go all the way down to the molecular level. In this paper, we discuss the role that AA derivatives might play during WD and nerve regeneration, and the therapeutic possibilities that arise.

  6. Arachidonic Acid Derivatives and Their Role in Peripheral Nerve Degeneration and Regeneration

    Science.gov (United States)

    Camara-Lemarroy, Carlos Rodrigo; Gonzalez-Moreno, Emmanuel Irineo; Guzman-de la Garza, Francisco Javier; Fernandez-Garza, Nancy Esthela

    2012-01-01

    After peripheral nerve injury, a process of axonal degradation, debris clearance, and subsequent regeneration is initiated by complex local signaling, called Wallerian degeneration (WD). This process is in part mediated by neuroglia as well as infiltrating inflammatory cells and regulated by inflammatory mediators such as cytokines, chemokines, and the activation of transcription factors also related to the inflammatory response. Part of this neuroimmune signaling is mediated by the innate immune system, including arachidonic acid (AA) derivatives such as prostaglandins and leukotrienes. The enzymes responsible for their production, cyclooxygenases and lipooxygenases, also participate in nerve degeneration and regeneration. The interactions between signals for nerve regeneration and neuroinflammation go all the way down to the molecular level. In this paper, we discuss the role that AA derivatives might play during WD and nerve regeneration, and the therapeutic possibilities that arise. PMID:22997489

  7. Evolution in medicinal chemistry of ursolic acid derivatives as anticancer agents.

    Science.gov (United States)

    Chen, Haijun; Gao, Yu; Wang, Ailan; Zhou, Xiaobin; Zheng, Yunquan; Zhou, Jia

    2015-03-06

    Currently, there is a renewed interest in common dietaries and plant-based traditional medicines for the prevention and treatment of cancer. In the search for potential anticancer agents from natural sources, ursolic acid (UA), a pentacyclic triterpenoid widely found in various medicinal herbs and fruits, exhibits powerful biological effects including its attractive anticancer activity against various types of cancer cells. However, the limited solubility, rapid metabolism and poor bioavailability of UA restricted its further clinical applications. In the past decade, with substantial progress toward the development of new chemical entities for the treatment of cancer, numerous UA derivatives have been designed and prepared to overcome its disadvantages. Despite extensive effort, discovery of effective UA derivatives has so far met with only limited success. This review summarizes the current status of the structural diversity and evolution in medicinal chemistry of UA analogues and provides a detailed discussion of future direction for further research in the chemical modifications of UA.

  8. Metformin inhibits Branched Chain Amino Acid (BCAA) derived ketoacidosis and promotes metabolic homeostasis in MSUD

    Science.gov (United States)

    S. Sonnet, Davis; N. O’Leary, Monique; A. Gutierrez, Mark; M. Nguyen, Steven; Mateen, Samiha; Hsu, Yuehmei; P. Mitchell, Kylie; J. Lopez, Antonio; Vockley, Jerry; K. Kennedy, Brian; Ramanathan, Arvind

    2016-01-01

    Maple Syrup Urine Disease (MSUD) is an inherited disorder caused by the dysfunction in the branched chain keto-acid dehydrogenase (BCKDH) enzyme. This leads to buildup of branched-chain keto-acids (BCKA) and branched-chain amino acids (BCAA) in body fluids (e.g. keto-isocaproic acid from the BCAA leucine), leading to numerous clinical features including a less understood skeletal muscle dysfunction in patients. KIC is an inhibitor of mitochondrial function at disease relevant concentrations. A murine model of intermediate MSUD (iMSUD) shows significant skeletal muscle dysfunction as by judged decreased muscle fiber diameter. MSUD is an orphan disease with a need for novel drug interventions. Here using a 96-well plate (liquid chromatography- mass spectrometry (LC-MS) based drug-screening platform we show that Metformin, a widely used anti-diabetic drug, reduces levels of KIC in patient-derived fibroblasts by 20–50%. This Metformin-mediated effect was conserved in vivo; Metformin-treatment significantly reduced levels of KIC in the muscle (by 69%) and serum (by 56%) isolated from iMSUD mice, and restored levels of mitochondrial metabolites (e.g. AMP and other TCA). The drug also decreased the expression of mitochondrial branched chain amino transferase (BCAT) which produces KIC in skeletal muscle. This suggests that Metformin can restore skeletal muscle homeostasis in MSUD by decreasing mitochondrial KIC production. PMID:27373929

  9. Metformin inhibits Branched Chain Amino Acid (BCAA) derived ketoacidosis and promotes metabolic homeostasis in MSUD.

    Science.gov (United States)

    S Sonnet, Davis; N O'Leary, Monique; A Gutierrez, Mark; M Nguyen, Steven; Mateen, Samiha; Hsu, Yuehmei; P Mitchell, Kylie; J Lopez, Antonio; Vockley, Jerry; K Kennedy, Brian; Ramanathan, Arvind

    2016-07-04

    Maple Syrup Urine Disease (MSUD) is an inherited disorder caused by the dysfunction in the branched chain keto-acid dehydrogenase (BCKDH) enzyme. This leads to buildup of branched-chain keto-acids (BCKA) and branched-chain amino acids (BCAA) in body fluids (e.g. keto-isocaproic acid from the BCAA leucine), leading to numerous clinical features including a less understood skeletal muscle dysfunction in patients. KIC is an inhibitor of mitochondrial function at disease relevant concentrations. A murine model of intermediate MSUD (iMSUD) shows significant skeletal muscle dysfunction as by judged decreased muscle fiber diameter. MSUD is an orphan disease with a need for novel drug interventions. Here using a 96-well plate (liquid chromatography- mass spectrometry (LC-MS) based drug-screening platform we show that Metformin, a widely used anti-diabetic drug, reduces levels of KIC in patient-derived fibroblasts by 20-50%. This Metformin-mediated effect was conserved in vivo; Metformin-treatment significantly reduced levels of KIC in the muscle (by 69%) and serum (by 56%) isolated from iMSUD mice, and restored levels of mitochondrial metabolites (e.g. AMP and other TCA). The drug also decreased the expression of mitochondrial branched chain amino transferase (BCAT) which produces KIC in skeletal muscle. This suggests that Metformin can restore skeletal muscle homeostasis in MSUD by decreasing mitochondrial KIC production.

  10. Effect of salicyclic acid on gluccorticoid receptor in cultured fibroblasts derived from rat carrageenin granuloma.

    Science.gov (United States)

    Koshihara, Y; Yamagishi, M; Murota, S I

    1976-06-23

    The binding activity of [3H]dexamethasone to the specific receptor was studied in the cytoplasmic fraction of a established fibroblast line derived from rat carrageenin granuloma in culture condition. Specific receptor to dexamethasone was demonstrated. Scatchard analysis revealed a single class of binding sites with a dissociation constant for [3H]dexamethasone of 3.64 - 10(-8) M and a concentration of binding sites of 0.825 pmol per mg cytosol protein. The number of cytoplasmic binding sites per cell was calculated at 1.15 - 10(5). Total binding activity to [3H]dexamethasone of the cytoplasmic fraction was enhanced when the cells were cultured in a medium containing salicylic acid was at 37 degrees C. The maximum enhancement was seen at the concentration of 10(-3)M and in 3h treatment of salicylic acid. This enhancement by salicylic acid was lost when cycloheximide was added to the culture medium at the same time. If salicyclic acid was added to the cell free system, it showed no effect on the binding activity. The other non-steroidal anti-inflammatory drugs; phenylbutazone and indomethacin,also enhanced the total binding activity to [3H]dexamethasone of the cytoplasmic fraction at the concentration of 2 - 10(-5) M and 2 - 10(-7) M, respectively.

  11. Modification of nucleic acids by azobenzene derivatives and their applications in biotechnology and nanotechnology.

    Science.gov (United States)

    Li, Jing; Wang, Xingyu; Liang, Xingguo

    2014-12-01

    Azobenzene has been widely used as a photoregulator due to its reversible photoisomerization, large structural change between E and Z isomers, high photoisomerization yield, and high chemical stability. On the other hand, some azobenzene derivatives can be used as universal quenchers for many fluorophores. Nucleic acid is a good candidate to be modified because it is not only the template of gene expression but also widely used for building well-organized nanostructures and nanodevices. Because the size and polarity distribution of the azobenzene molecule is similar to a nucleobase pair, the introduction of azobenzene into nucleic acids has been shown to be an ingenious molecular design for constructing light-switching biosystems or light-driven nanomachines. Here we review recent advances in azobenzene-modified nucleic acids and their applications for artificial regulation of gene expression and enzymatic reactions, construction of photoresponsive nanostructures and nanodevices, molecular beacons, as well as obtaining structural information using the introduced azobenzene as an internal probe. In particular, nucleic acids bearing multiple azobenzenes can be used as a novel artificial nanomaterial with merits of high sequence specificity, regular duplex structure, and high photoregulation efficiency. The combination of functional groups with biomolecules may further advance the development of chemical biotechnology and biomolecular engineering.

  12. Production of fumaric acid from biodiesel-derived crude glycerol by Rhizopus arrhizus.

    Science.gov (United States)

    Zhou, Yuqing; Nie, Kaili; Zhang, Xin; Liu, Shihong; Wang, Meng; Deng, Li; Wang, Fang; Tan, Tianwei

    2014-07-01

    This work investigated the capability of Rhizopus arrhizus to assimilate biodiesel-derived crude glycerol and convert it into fumaric acid. After optimizing the initial glycerol concentration, spore inoculum and yeast extract concentration, smaller pellets (0.7 mm) and higher biomass (3.11 g/L) were obtained when R. arrhizus grew on crude glycerol. It was found that crude glycerol was more suitable than glucose for smaller R. arrhizus pellet forming. When 80 g/L crude glycerol was used as carbon source, the fumaric acid production of 4.37 g/L was obtained at 192 h. With a highest concentration of 22.81 g/L achieved in the co-fermentation of crude glycerol (40 g/L) and glucose (40 g/L) at 144 h, the fumaric acid production was enhanced by 553.6%, compared to the fermentation using glycerol (80 g/L) as sole carbon source. Moreover, the production cost of fumaric acid in co-fermentation was reduced by approximately 14% compared to glucose fermentation.

  13. Synthesis and Biological Activity of Arylspiroborate Salts Derived from Caffeic Acid Phenethyl Ester

    Directory of Open Access Journals (Sweden)

    Martin J. G. Hébert

    2015-01-01

    Full Text Available Two novel boron compounds containing caffeic acid phenethyl ester (CAPE derivatives have been prepared and characterized fully. These new compounds and CAPE have been investigated for potential antioxidant and antimicrobial properties and their ability to inhibit 5-lipoxygenase and whether chelation to boron improves their biological activity. Sodium salt 4 was generally more active than ammonium salt 5 in the biological assays and surpassed the radical scavenging ability of CAPE. Compounds 4 and 5 were more active than CAPE and Zileuton in human polymorphonuclear leukocytes. These results clearly show the effectiveness of the synthesized salts as transporter of CAPE.

  14. N-Hydroxypyrazolyl glycine derivatives as selective N-methyl-D-aspartic acid receptor ligands

    DEFF Research Database (Denmark)

    Clausen, Rasmus Prætorius; Christensen, Caspar; Hansen, Kasper Bø;

    2008-01-01

    A series of analogues based on N-hydroxypyrazole as a bioisostere for the distal carboxylate group of aspartate have been designed, synthesized, and pharmacologically characterized. Affinity studies on the major glutamate receptor subgroups show that these 4-substituted N-hydroxypyrazol-5-yl...... glycine (NHP5G) derivatives are selectively recognized by N-methyl- d-aspartic acid (NMDA) receptors and that the ( R)-enantiomers are preferred. Moreover, several of the compounds are able to discriminate between individual subtypes among the NMDA receptors, providing new pharmacological tools...

  15. Sesquiterpenes, flavonoids, shikimic acid derivatives and pyrrolizidine alkaloids from Senecio kingii Hook.

    Science.gov (United States)

    Ruiz-Vásquez, Liliana; Reina, Matías; López-Rodríguez, M; Giménez, Cristina; Cabrera, Raimundo; Cuadra, Pedro; Fajardo, Víctor; González-Coloma, Azucena

    2015-09-01

    Twenty-four compounds including eleven eremophilanolides (1-11), one eremophilane (13), five shikimic acid derivatives (14-18), six flavonoids (19-24), and the macrocyclic unsaturated pyrrolizidine alkaloid integerrimine (25) were isolated from Senecio kingii, an endemic species from the Magallanes Region (Chile). Compounds 3, 5, 6, 8-11 and 13-18 have not been previously reported as natural products. Their molecular structures were determined by NMR spectroscopic analysis and comparison with published NMR data. An X-ray-analysis of compound 3 has been performed. Their insecticidal and antifungal activities were tested, being compound 3 the strongest insect antifeedant. Compounds 6, 9 and 18 were moderate antifungals.

  16. Antitumor Mechanisms of Amino Acid Hydroxyurea Derivatives in the Metastatic Colon Cancer Model

    Directory of Open Access Journals (Sweden)

    Nina Šaban

    2013-12-01

    Full Text Available The paper presents a detailed study of the biological effects of two amino acid hydroxyurea derivatives that showed selective antiproliferative effects in vitro on the growth of human tumor cell line SW620. Tested compounds induced cell cycle perturbations and apoptosis. Proteins were identified by proteomics analyses using two-dimensional gel electrophoresis coupled to mass spectrometry, which provided a complete insight into the most probable mechanism of action on the protein level. Molecular targets for tested compounds were analyzed by cheminformatics tools. Zinc-dependent histone deacetylases were identified as potential targets responsible for the observed antiproliferative effect.

  17. Polycarboxylate derivative of -amino acid as growth modifier of sulphide minerals

    Indian Academy of Sciences (India)

    Harjyoti Thakuria; Gopal Das

    2011-02-01

    Construction of modified inorganic mineral with controlled mineralization analogues of those produced by nature is now of current interest for understanding the mechanism of the in vivo biomineralization processes, as well as looking for fresh industrial and technological applications. Low-molecular-weight chiral polycarboxylate ligands derived fromnaturally occurring -\\alpha-amino acids have been used asmodel systems to study the effect of small organic matrix on crystal growth modification. The sulphide minerals are characterized by PXRD, FT–IR and SEM. Furthermore, the optical properties of these minerals have been characterized by UV-Vis and photoluminescence (PL) spectra.

  18. Amino acid anthranilamide derivatives as a new class of glycogen phosphorylase inhibitors.

    Science.gov (United States)

    Evans, Karen A; Li, Yue H; Coppo, Frank T; Graybill, Todd L; Cichy-Knight, Maria; Patel, Mehul; Gale, Jennifer; Li, Hu; Thrall, Sara H; Tew, David; Tavares, Francis; Thomson, Stephen A; Weiel, James E; Boucheron, Joyce A; Clancy, Daphne C; Epperly, Andrea H; Golden, Pamela L

    2008-07-15

    A series of amino acid anthranilamide derivatives identified from a high-throughput screening campaign as novel, potent, and glucose-sensitive inhibitors of human liver glycogen phosphorylase a are described. A solid-phase synthesis using Wang resin was also developed which provided efficient access to a variety of analogues, and resulted in the identification of key structure-activity relationships, and the discovery of a potent exemplar (IC(50)=80 nM). The SAR scope, synthetic strategy, and in vitro results for this series are presented herein.

  19. Dehydroabietic Acid Derivative QC4 Induces Gastric Cancer Cell Death via Oncosis and Apoptosis

    Directory of Open Access Journals (Sweden)

    Dongjun Luo

    2016-01-01

    Full Text Available Aim. QC4 is the derivative of rosin’s main components dehydroabietic acid (DHA. We investigated the cytotoxic effect of QC4 on gastric cancer cells and revealed the mechanisms beneath the induction of cell death. Methods. The cytotoxic effect of QC4 on gastric cancer cells was evaluated by CCK-8 assay and flow cytometry. The underlying mechanisms were tested by administration of cell death related inhibitors and detection of apoptotic and oncosis related proteins. Cytomembrane integrity and organelles damage were confirmed by lactate dehydrogenase (LDH leakage assay, mitochondrial function test, and cytosolic free Ca2+ concentration detection. Results. QC4 inhibited cell proliferation dose- and time-dependently and destroyed cell membrane integrity, activated calpain-1 autolysis, and induced apoptotic protein cleavage in gastric cancer cells. The detection of decreased ATP and mitochondrial membrane potential, ROS accumulation, and cytosolic free Ca2+ elevation confirmed organelles damage in QC4-treated gastric cancer cells. Conclusions. DHA derivative QC4 induced the damage of cytomembrane and organelles which finally lead to oncosis and apoptosis in gastric cancer cells. Therefore, as a derivative of plant derived small molecule DHA, QC4 might become a promising agent in gastric cancer therapy.

  20. Comparative reactivity of the myeloperoxidase-derived oxidants hypochlorous acid and hypothiocyanous acid with human coronary artery endothelial cells.

    Science.gov (United States)

    Lloyd, Mitchell M; Grima, Michael A; Rayner, Benjamin S; Hadfield, Katrina A; Davies, Michael J; Hawkins, Clare L

    2013-12-01

    In the immune response, hypohalous acids are generated by activated leukocytes via the release of myeloperoxidase and the formation of H2O2. Although these oxidants have important bactericidal properties, they have also been implicated in causing tissue damage in inflammatory diseases, including atherosclerosis. Hypochlorous acid (HOCl) and hypothiocyanous acid (HOSCN) are the major oxidants formed by myeloperoxidase under physiological conditions, with the ratio of these oxidants dependent on diet and smoking status. HOCl is highly reactive and causes marked cellular damage, but few data are available on the effects of HOSCN on mammalian cells. In this study, we have compared the actions of HOCl and HOSCN on human coronary artery endothelial cells (HCAEC). HOCl reacts rapidly with the cells, resulting in extensive cell death by both apoptosis and necrosis, with necrosis dominating at higher oxidant doses. In contrast, HOSCN is consumed more slowly, with cell death occurring only by apoptosis. Exposure of HCAEC to HOCl and HOSCN induces changes in mitochondrial membrane permeability, which, in the case of HOSCN, is associated with mitochondrial release of proapoptotic factors, including cytochrome c, apoptosis-inducing factor, and endonuclease G. With each oxidant, apoptosis appears to be caspase-independent, with the inactivation of caspases 3/7 observed, and pretreatment of the cells with the caspase inhibitor Z-VAD-fmk having no effect on the extent of cell death. Loss of cellular thiols, depletion of glutathione, and the inactivation of thiol-dependent enzymes, including glyceraldehyde-3-phosphate dehydrogenase, were seen with both oxidants, though to a much greater extent with HOCl. The ability of myeloperoxidase-derived oxidants to induce endothelial cell apoptosis may contribute to the formation of unstable lesions in atherosclerosis. The results with HOSCN may be particularly significant for smokers, who have elevated plasma levels of SCN(-), the precursor

  1. In vivo pharmacokinetics, biodistribution and antitumor effect of amphiphilic poly(L-amino acids) micelles loaded with a novel all-trans retinoic acid derivative.

    Science.gov (United States)

    Tang, Jihui; Wang, Xinqun; Wang, Ting; Chen, Feihu; Zhou, Jianping

    2014-01-23

    Poly(amino acid)s are well-known as biodegradable and environmentally acceptable materials. In this study, a series of poly(L-aspartic acid)-b-poly(L-phenylalanine) (PAA-PPA) compounds with different degrees of polymerization were used to prepare copolymer micelles for a poorly water-soluble drug 4-amino-2-trifluoromethyl-phenyl retinate (ATPR, a novel all-trans retinoic acid derivative) and in vivo pharmacokinetics, biodistribution and antitumor efficacy of ATPR delivered by PAA-PPA micelles were evaluated. The area under the plasma concentration time curve AUC0→∞ of ATPR-loaded PAA20PPA20 micelles was 2.23 and 1.97 times higher than that of ATPR solution and ATPR CrmEL solution, respectively; In addition, the mean residence time (MRT) was increased 1.67 and 1.97-fold, respectively and the total body clearance (CL) was reduced 2.25 and 1.98-fold, respectively. The biodistribution study indicated that most of the ATPR in the ATPR-M group was distributed in the liver and there was delayed liver aggregation compared with the ATPR solution and ATPR CrmEL solution groups. Furthermore, the antitumor efficacy of ATPR-loaded PAA20PPA20 micelles was demonstrated in in vivo antitumor models involving mice inoculated with the human gastric cancer cell line SGC-7901. At the same dose of 7mg/kg, the ATPR-loaded micelles group demonstrated a better tumor growth inhibition and induced differentiation than the groups given ATPR solution and ATPR CrmEL solution. Therefore, the ATPR-loaded PAA-PPA micelles appear to be a potentially useful drug delivery system for ATPR and suitable for the chemotherapy of gastric cancer.

  2. Facile Synthesis of Monofluoro y-Lactones and Pyrrolidine Derivatives via Electrophilic Fluorination of Allenoic Acids and Amides

    Institute of Scientific and Technical Information of China (English)

    CUl Haifeng; CHAI Zhuo; ZHAO Gang; ZHU Shizheng

    2009-01-01

    A convenient method to synthesize a series of monofluoro γ-1actones and pyrrolidine derivatives in moderate to good yields via the electrophilic fluorination of y-allenoic acids and tosylamides using Selectfluor was developed.

  3. The marine sponge-derived polyketide endoperoxide plakortide F acid mediates its antifungal activity by interfering with calcium homeostasis

    Science.gov (United States)

    Plakortide F acid (PFA) is a marine-derived polyketide endoperoxide exhibiting strong inhibitory activity against several clinically important fungal pathogens. In the present study, transcriptional profiling coupled with mutant and biochemical analyses were conducted using the model organism Sacch...

  4. Effective synthesis of optically active trifluoromethyldiazirinyl homophenylalanine and aroylalanine derivatives with the Friedel-Crafts reaction in triflic acid.

    Science.gov (United States)

    Murashige, Ryo; Murai, Yuta; Hatanaka, Yasumaru; Hashimoto, Makoto

    2009-06-01

    The Friedel-Crafts reaction with 3-(3-methoxyphenyl)-3-(trifluoromethyl)-3H-diazirine and optically active N-TFA-Asp(Cl)-OMe in triflic acid afforded homophenylalanine derivatives without any loss of the optical purity.

  5. Immunotoxic effects of oil sands-derived naphthenic acids to rainbow trout

    Energy Technology Data Exchange (ETDEWEB)

    MacDonald, Gillian Z.; Hogan, Natacha S. [Canadian Rivers Institute, Department of Biology, University of Prince Edward Island, 550 University Avenue, Charlottetown, PEI (Canada); Koellner, Bernd [Friedrich Loeffler Institute, Federal Research Institute of Animal Health, Institute of Immunology, Greifswald (Germany); Thorpe, Karen L.; Phalen, Laura J. [Canadian Rivers Institute, Department of Biology, University of Prince Edward Island, 550 University Avenue, Charlottetown, PEI (Canada); Wagner, Brian D. [Department of Chemistry, University of Prince Edward Island, Charlottetown (Canada); Heuvel, Michael R. van den, E-mail: mheuvel@upei.ca [Canadian Rivers Institute, Department of Biology, University of Prince Edward Island, 550 University Avenue, Charlottetown, PEI (Canada)

    2013-01-15

    Naphthenic acids are the major organic constituents in waters impacted by oil sands. To investigate their immunotoxicity, rainbow trout (Oncorhynchus mykiss) were injected with naphthenic acids extracted from aged oil sands tailings water. In two experiments, rainbow trout were injected intraperitoneally with 0, 10, or 100 mg/kg of naphthenic acids, and sampled after 5 or 21 d. Half of the fish from the 21 d exposure were co-exposed to inactivated Aeromonas salmonicida (A.s.) to induce an immune response. A positive control experiment was conducted using an intraperitoneal injection of 100 mg/kg of benzo[a]pyrene, a known immune suppressing compound. T-lymphocytes, B-lymphocytes, thrombocytes, and myeloid cells were counted in blood and lymphatic tissue using flow cytometry. In the 5 d exposure, there was a reduction in blood leucocytes and spleen thrombocytes at the 100 mg/kg dose. However, at 21 d, leucocyte populations showed no effects of exposure with the exception that spleen thrombocyte populations increase at the 100 mg/kg dose. In the 21 d exposure, B- and T-lymphocytes in blood showed a significant Dose Multiplication-Sign A.s. interaction, indicating stimulated blood cell proliferation due to naphthenic acids alone as well as due to A.s. Naphthenic acid injections did not result in elevated bile fluorescent metabolites or elevated hepatic EROD activity. In contrast to naphthenic acids exposures, as similar dose of benzo[a]pyrene caused a significant decrease in B- and T-lymphocyte absolute counts in blood and relative B-lymphocyte counts in spleen. Results suggest that the naphthenic acids may act via a generally toxic mechanism rather than by specific toxic effects on immune cells.

  6. The Use of Serum Uric Acid Concentration as an Indicator of Laparoscopic Sleeve Gastrectomy Success

    Science.gov (United States)

    Menenakos, Evangelos; Doulami, Georgia; Tzanetakou, Irene P.; Natoudi, Maria; Kokoroskos, Nikolaos; Almpanopoulos, Konstantinos; Leandros, Emmanouil; Zografos, George; Theodorou, Dimitrios

    2015-01-01

    Laparoscopic sleeve gastrectomy (LSG) effectively reduces weight by restricting gastric capacity and altering gut hormones levels. We designed a prospective study to investigate the correlation of serum uric acid (SUA) concentration and weight loss. SUA and body mass index (BMI) were measured preoperatively and on first postoperative month and year in patients who underwent LSG in our department of bariatric surgery. Data on 55 patients were analyzed. Preoperative SUA concentration had a significant positive correlation with percentage of total weight loss (TWL) on first postoperative month (P = 0.001) and year (P = 0.002). SUA concentration on first postoperative month had a positive correlation with percentage of TWL on first postoperative year (P = 0.004). SUA concentration could be used as a predictor of LSG's success and could help in early detection of patients with rapid loss of weight, in order to prevent complications. PMID:25594659

  7. Synthesis and Antiproliferative Activity of Some Novel Triazole Derivatives from Dehydroabietic Acid

    Directory of Open Access Journals (Sweden)

    Mariano Walter Pertino

    2014-02-01

    Full Text Available Dehydroabietic acid (DHA is a naturally occurring diterpene with different and relevant biological activities. Previous studies have shown that some DHA derivatives display antiproliferative activity. However, the reported compounds did not include triazole derivatives. Starting from DHA (8,11,13-abietatrien-18-oic acid, and its alcohol dehydroabietinol (8,11,13-abietatrien-18-ol, four alkyl esters were prepared. The alkyl terpenes were treated with different aromatic azides to synthesize hybrid compounds using click chemistry. Some 16 new DHA hybrids were thus synthesized and their structures were confirmed by spectroscopic and spectrometric means. The antiproliferative activity of the new compounds was assessed towards human cell lines, namely normal lung fibroblasts (MRC-5, gastric epithelial adenocarcinoma (AGS, lung cancer (SK-MES-1 and bladder carcinoma (J82 cells. Better antiproliferative effect was found for compound 5, with an IC50 of 6.1 μM and selectivity on SK-MES-1 cells. Under the same experimental conditions, the IC50 of etoposide, was 1.83 µM.

  8. Dehydroabietic Acid Derivative QC2 Induces Oncosis in Hepatocellular Carcinoma Cells

    Directory of Open Access Journals (Sweden)

    Guang Zhang

    2014-01-01

    Full Text Available Aim. Rosin, the traditional Chinese medicine, is reported to be able to inhibit skin cancer cell lines. In this report, we investigate the inhibitory effect against HCC cells of QC2, the derivative of rosin’s main components dehydroabietic acid. Methods. MTT assay was used to determine the cytotoxicity of QC2. Morphological changes were observed by time-lapse microscopy and transmission electron microscopy and the cytoskeleton changes were observed by laser-scanning confocal microscopy. Cytomembrane integrity and organelles damage were confirmed by detection of the reactive oxygen (ROS, lactate dehydrogenase (LDH, and mitochondrial membrane potential (Δψm. The underlying mechanism was manifested by Western blotting. The oncotic cell death was further confirmed by detection of oncosis related protein calpain. Results. Swelling cell type and destroyed cytoskeleton were observed in QC2-treated HCC cells. Organelle damage was visualized by transmission electron microscopy. The detection of ROS accumulation, increased LDH release, and decreased ATP and Δψm confirmed the cell death. The oncotic related protein calpain was found to increase time-dependently in QC2-treated HCC cells, while its inhibitor PD150606 attenuated the cytotoxicity. Conclusions. Dehydroabietic acid derivative QC2 activated oncosis related protein calpain to induce the damage of cytomembrane and organelles which finally lead to oncosis in HCC cells.

  9. Synthesis of ino Acid Derived β-Cyclodextrins Used in Chiral Separation by Capillary Electrophoresis

    Institute of Scientific and Technical Information of China (English)

    戴荣继; 佟斌; 魏征; 顾峻岭; 邓玉林; 李明愉; 傅若农

    2004-01-01

    Six new kinds of ino acid derived β-cyclodextrins were synthesized to improve their water solubility and chiral separation properties. They are heptakis{2,6-di-O-[3-L-(1-isopropyl carboxyl methyl ino)-2-hydroxy propyl]}-β-cyclodextrin (i.e. L-Val-β-CD), heptakis{2,6-di-O-[3-L-(1-benzyl carboxyl methyl ino)-2-hydroxy propyl]}-β-cyclodextrin (i.e. L-Phe-β-CD), heptakis{2,6-di-O-[3-(D, L-1-benzyl carboxyl methyl ino)-2-hydroxy propyl]}-β-cyclodextrin (i.e. D,L-Phe-β-CD), heptakis{2,6-di-O-[3-(L-1-hydroxymethyl carboxyl methyl ino)-2-hydroxy propyl]}-β-cyclodextrin (i.e. L-Ser-β-CD), heptakis{2,6-di-O-[3-(L-1-carboxylmethyl carboxyl methyl ino)- 2-hydroxy propyl]}-β-cyclodextrin (i.e. L-Asp-β-CD), heptakis{2,6-di-O-[3-(L-2-carboxyl tetrethylene ino)-2-hydroxy propyl]}-β-cyclodextrin (i.e. L-Pro-β-CD). Their chemical structures were certified using FTIR and 1H NMR. Except for L-Phe-β-CD and D,L-Phe-β-CD, that are in soluble in water, the other ino acid derived β-CDs all have good water solubility. D,L-tyrosine and promethazine were baselinely separated by L-Val-β-CD in capillary electrophoresis.

  10. Synthesis, spectroscopic characterizations, crystal structures and DFT studies of nalidixic acid carbonyl hydrazones derivatives

    Science.gov (United States)

    Bergamini, F. R. G.; Ribeiro, M. A.; Lancellotti, M.; Machado, D.; Miranda, P. C. M. L.; Cuin, A.; Formiga, A. L. B.; Corbi, P. P.

    2016-09-01

    This article describes the synthesis and characterization of the 1-ethyl-7-methyl-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carbohydrazide (hzd) and six carbonyl hydrazones derivatives of the nalidixic with 1H-pyrrol-2-ylmethylidene (hpyrr), 1H-imidazol-2-ylmethylidene (h2imi), pyridin-2-ylmethylidene (h2py), pyridin-3-ylmethylidene (h3py), pyridin-4-ylmethylidene(h4py) and (2-hydroxyphenyl)methylidene (hsali). The carbonyl hydrazones were characterized by elemental and ESI-QTOF-MS analyses, IR and detailed NMR spectroscopic measurements. The 2D NMR experiments allowed the unambiguous assignment of the hydrogen, carbon and nitrogen atoms, which have not been reported for nalidixic acid carbonyl hydrazone derivatives so far. Crystal structures of hzd and the new carbonyl hydrazones h2imi, hpyrr and h3py were determined by X-ray diffraction studies. Although the synthesis of hzd was reported decades ago, the hzd crystal structure have not been reported yet. Geometric optimizations of all the characterized structures were performed with the aid of DFT studies. Despite the fact that the hydrazones with 2-pyridine carboxylic acid (h2py) and salicyl aldehyde (hsali) were already reported by literature, a detailed spectroscopic study followed by DFT studies are also reported for such compounds in this manuscript. Antimicrobial studies of the compounds are also presented.

  11. Modification of the cellulosic component of hemp fibers using sulfonic acid derivatives: Surface and thermal characterization.

    Science.gov (United States)

    George, Michael; Mussone, Paolo G; Bressler, David C

    2015-12-10

    The aim of this study was to characterize the surface, morphological, and thermal properties of hemp fibers treated with two commercially available, inexpensive, and water soluble sulfonic acid derivatives. Specifically, the cellulosic component of the fibers were targeted, because cellulose is not easily removed during chemical treatment. These acids have the potential to selectively transform the surfaces of natural fibers for composite applications. The proposed method proceeds in the absence of conventional organic solvents and high reaction temperatures. Surface chemical composition and signature were measured using gravimetric analysis, X-ray photoelectron spectroscopy (XPS) and Fourier transform infra-red spectroscopy (FTIR). XPS data from the treated hemp fibers were characterized by measuring the reduction in O/C ratio and an increase in abundance of the C-C-O signature. FTIR confirmed the reaction with the emergence of peaks characteristic of disubstituted benzene and amino groups. Grafting of the sulfonic derivatives resulted in lower surface polarity. Thermogravimetric analysis revealed that treated fibers were characterized by lower percent degradation between 200 and 300 °C, and a higher initial degradation temperature.

  12. Reducing Renal Uptake of {sup 177}Lu Labeled CCK Derivative using Basic Amino Acids

    Energy Technology Data Exchange (ETDEWEB)

    Lee, Soyoung; Lim, Jaecheong; Joh, Eunha [Korea Atomic Energy Research Institute, Daejeon (Korea, Republic of)

    2014-05-15

    Radiolabeled peptides have been designed to target the relative receptors overespressed in tumor cells, such as integrin αvβ3, gastrin-releasing peptide receptor (GRPR), melanocortin-1 receptor (MC1-R), glucagon-like peptide-a receptor (GLP-1R), and cholecystokinin (CCK) receptor. Most of these peptides are eliminated from the body via the kidney and are partly reabsorbed in the proximal tubular cells. However, the high renal uptake of the radiolabeled peptides may lead to renal toxicity. In this study we investigated various amino acid solutions to reduce the renal uptake of {sup 177}Lu-DOTA-CCK derivative. Renal uptake of {sup 177}Lu-DOTA-CCK derivative is effectively reduced by the administration of positively charged amino acids. The administration of 12 mg of L-lysine was as effective in reducing the renal uptake as 6 mg of lysine and 6 mg of arginine combinations. Further studies will be performed to identify the most potent inhibitor of renal reuptake of radiolabeled peptides and minimize the chance of unwanted side effects.

  13. 11-Oxoeicosatetraenoic acid is a cyclooxygenase-2/15-hydroxyprostaglandin dehydrogenase-derived antiproliferative eicosanoid.

    Science.gov (United States)

    Liu, Xiaojing; Zhang, Suhong; Arora, Jasbir S; Snyder, Nathaniel W; Shah, Sumit J; Blair, Ian A

    2011-12-19

    Previously, we established that 11(R)-hydroxy-5,8,12,14-(Z,Z,E,Z)-eicosatetraenoic acid (HETE) was a significant cyclooxygenase (COX)-2-derived arachidonic acid (AA) metabolite in epithelial cells. Stable isotope dilution chiral liquid chromatography (LC)-electron capture atmospheric pressure chemical ionization (ECAPCI)/mass spectrometry (MS) was used to quantify COX-2-derived eicosanoids in the human colorectal adenocarcinoma (LoVo) epithelial cell line, which expresses both COX-2 and 15-hydroxyprostaglandin dehydrogenase (15-PGDH). 11(R)-HETE secretion reached peak concentrations within minutes after AA addition before rapidly diminishing, suggesting further metabolism had occurred. Surprisingly, recombinant 15-PGDH, which is normally specific for oxidation of eicosanoid 15(S)-hydroxyl groups, was found to convert 11(R)-HETE to 11-oxo-5,8,12,14-(Z,Z,E,Z)-eicosatetraenoic acid (ETE). Furthermore, LoVo cell lysates converted 11(R)-HETE to 11-oxo-ETE and inhibition of 15-PGDH with 5-[[4-(ethoxycarbonyl)phenyl]azo]-2-hydroxy-benzeneacetic acid (CAY10397) (50 μM) significantly suppressed endogenous 11-oxo-ETE production with a corresponding increase in 11(R)-HETE. These data confirmed COX-2 and 15-PGDH as enzymes responsible for 11-oxo-ETE biosynthesis. Finally, addition of AA to the LoVo cells resulted in rapid secretion of 11-oxo-ETE into the media, reaching peak levels within 20 min of starting the incubation. This was followed by a sharp decrease in 11-oxo-ETE levels. Glutathione (GSH) S-transferase (GST) was found to metabolize 11-oxo-ETE to the 11-oxo-ETE-GSH (OEG)-adduct in LoVo cells, as confirmed by LC-MS/MS analysis. Bromodeoxyuridine (BrdU)-based cell proliferation assays in human umbilical vein endothelial cells (HUVECs) revealed that the half-maximal inhibitory concentration (IC(50)) of 11-oxo-ETE for inhibition of HUVEC proliferation was 2.1 μM. These results show that 11-oxo-ETE is a novel COX-2/15-PGDH-derived eicosanoid, which inhibits endothelial

  14. Thermogenesis, blood metabolites and hormones, and growth of lambs born to ewes supplemented with algae-derived docosahexaenoic acid.

    Science.gov (United States)

    Keithly, J I; Kott, R W; Berardinelli, J G; Moreaux, S; Hatfield, P G

    2011-12-01

    Neonatal lamb mortality is a major factor affecting profitability in the sheep industry, and lamb thermogenesis is a key element in neonatal lamb survival. Increased lamb vigor has been reported when ewes were supplemented during late gestation with algae-derived docosahexaenoic acid (DHA); however, the effects of DHA on lamb thermogenesis and immunocompetence have not been investigated. Eighty twin-bearing Targhee ewes (ages 2 to 5 yr; 68.5 ± 3 kg) were assigned randomly to 1 of 2 supplement treatments to determine the effects of feeding DHA to ewes during late gestation and early lactation on lamb thermogenesis, serum metabolites and hormones, and lamb growth. Supplement treatments were 12 g·ewe(-1)·d(-1) of algae-derived DHA (DHA Gold Advanced Bionutrition Corp., Columbia, MD; algae-derived DHA); and no algae-derived DHA (control). Supplements were individually fed daily during the last 30 d (±7 d) of gestation and pen fed (6 pens/treatment with 6 or 7 ewes/pen) during the first 38 d (±7 d) of lactation. One hour after lambing and before nursing, twin-born lambs were weighed, blood sampled via jugular puncture, and placed in a dry cold chamber for 30 min (0°C), and rectal temperatures were recorded every minute for 30 min. Lambs were removed from the cold chamber, blood sampled, warmed for 15 min, and returned to their dam. Ewes were blood sampled, and colostrum samples were collected 1 h postpartum. Ewe and lamb sera were assayed for glucose, NEFA, cortisol, and leptin. Lamb rectal temperature, glucose, NEFA, cortisol, leptin, and birth weights did not differ between treatments. The BW at 38 d was greater (P = 0.03) for lambs born to control ewes than for lambs born to algae-derived DHA-supplemented ewes; however, the colostrum of algae-derived DHA-supplemented ewes had a greater specific gravity (P = 0.05) than for control ewes. Overall, despite a potentially positive effect on ewe colostral IgG concentrations, supplementation of algae-derived DHA during

  15. Synthesis and structural characterization of derivatives of 2- and 3-benzo[b]furan carboxylic acids with potential cytotoxic activity.

    Science.gov (United States)

    Kossakowski, Jerzy; Ostrowska, Kinga; Hejchman, Elzbieta; Wolska, Irena

    2005-01-01

    Derivatives of 2- and 3-benzo[b]furancarboxylic acids were prepared and evaluated for their cytotoxic potential in the National Cancer Institute, Bethesda, USA. Six compounds: 7-acetyl-6-hydroxy-3-methyl-2-benzofurancarboxylic acid (2), 6-hydroxy-7-(p-methoxycinnamoyl)-3-methyl-2-benzofurancarboxylic acid (4), 5-bromo-7-hydroxy-6-methoxy-2-benzofurancarboxylic acid methyl ester (6a), 6-acetyl-5-(O-ethyl-2'-diethylamino)-2-methyl-3-benzofurancarboxylic acid methyl ester (1f), 6-(O-ethyl-2'-diethylamino)-7-p-methoxycinnamoyl)-3-methyl-2-benzofurancarboxylic acid methyl ester hydrochloride (4b), 5-bromo-7-(O-ethyl-2'-diethylamino)-6-methoxy-2-benzofurancarboxylic acid methyl ester (6b) showed significant cytotoxic activities against human cancer cell lines. In addition the crystal structures of 7-methoxy-2-benzofurancarboxylic acid methyl ester (7a) has been solved by X-ray structure analysis of single crystals.

  16. Removal of aqueous oxalic acid by heterogeneous catalytic ozonation with MnOx/sewage sludge-derived activated carbon as catalysts.

    Science.gov (United States)

    Huang, Yuanxing; Sun, Yaru; Xu, Zhihua; Luo, Mengyu; Zhu, Chunlei; Li, Liang

    2017-01-01

    MnOx/sewage sludge-derived activated carbon (MnOx/SAC) was prepared as catalysts to improve the performance of aqueous oxalic acid degradation by ozonation. The results indicated that MnOx/SAC had excellent catalytic activity in mineralization of oxalic acid during heterogeneous catalytic ozonation process. MnOx/SAC with a manganese load of 30% exhibited the strongest catalytic activity under the condition of solution pH3.5, which enhanced the oxalic acid removal from 10.3% to 92.2% in 60min compared with that treated by ozone alone. Increase of catalyst dosage and aqueous ozone concentration was advantageous for oxalic acid removal from water. On the basis of catalyst characterization analysis and the observation of inhibitory effect induced by higher pH, less catalyst dosage as well as the presence of hydroxyl radical scavenger, it was deduced that the reaction mechanism involved both hydroxyl radicals attack and surface reactions.

  17. THE "CHEMICAL OXYGEN DEMAND / TOTAL VOLATILE ACIDS" RATIO AS AN ANAEROBIC TREATABILITY INDICATOR FOR LANDFILL LEACHATES

    OpenAIRE

    Contrera,R. C.; K. C. da Cruz Silva; G. H. Ribeiro Silva; D. M. Morita; Zaiat,M.; V. Schalch

    2015-01-01

    Abstract In some operational circumstances a fast evaluation of landfill leachate anaerobic treatability is necessary, and neither Biochemical Methane Potential nor BOD/COD ratio are fast enough. Looking for a fast indicator, this work evaluated the anaerobic treatability of landfill leachate from São Carlos-SP (Brazil) in a pilot scale Anaerobic Sequence Batch Biofilm Reactor (AnSBBR). The experiment was conducted at ambient temperature in the landfill area. After the acclimation, at a ...

  18. Host-Derived Sialic Acids Are an Important Nutrient Source Required for Optimal Bacterial Fitness In Vivo

    Directory of Open Access Journals (Sweden)

    Nathan D. McDonald

    2016-04-01

    Full Text Available A major challenge facing bacterial intestinal pathogens is competition for nutrient sources with the host microbiota. Vibrio cholerae is an intestinal pathogen that causes cholera, which affects millions each year; however, our knowledge of its nutritional requirements in the intestinal milieu is limited. In this study, we demonstrated that V. cholerae can grow efficiently on intestinal mucus and its component sialic acids and that a tripartite ATP-independent periplasmic SiaPQM strain, transporter-deficient mutant NC1777, was attenuated for colonization using a streptomycin-pretreated adult mouse model. In in vivo competition assays, NC1777 was significantly outcompeted for up to 3 days postinfection. NC1777 was also significantly outcompeted in in vitro competition assays in M9 minimal medium supplemented with intestinal mucus, indicating that sialic acid uptake is essential for fitness. Phylogenetic analyses demonstrated that the ability to utilize sialic acid was distributed among 452 bacterial species from eight phyla. The majority of species belonged to four phyla, Actinobacteria (members of Actinobacillus, Corynebacterium, Mycoplasma, and Streptomyces, Bacteroidetes (mainly Bacteroides, Capnocytophaga, and Prevotella, Firmicutes (members of Streptococcus, Staphylococcus, Clostridium, and Lactobacillus, and Proteobacteria (including Escherichia, Shigella, Salmonella, Citrobacter, Haemophilus, Klebsiella, Pasteurella, Photobacterium, Vibrio, and Yersinia species, mostly commensals and/or pathogens. Overall, our data demonstrate that the ability to take up host-derived sugars and sialic acid specifically allows V. cholerae a competitive advantage in intestinal colonization and that this is a trait that is sporadic in its occurrence and phylogenetic distribution and ancestral in some genera but horizontally acquired in others.

  19. An efficient way to coupling amine with derivatives of steric N-Boc-pyrrolidine-2-carboxylic acid

    Institute of Scientific and Technical Information of China (English)

    Feng Zhi Liu; Hao Fang; Wen Fang Xu

    2007-01-01

    An efficient way to coupling amine with the derivatives of steric N-Boc-pyrrolidine-2-carboxylic acid was reported in this paper.We have found that the synthesis of derivatives is problematic with the commonly used DCC/HOBT method. As a substitute, the mixed anhydride method was adopted. A series of 6-(3-nitroguanidino)hexanamidopyrrolidine derivatives were prepared with this method.

  20. Lanthanide nitrates as Lewis acids in the one-pot synthesis of 1,2,4-oxadiazole derivatives

    Energy Technology Data Exchange (ETDEWEB)

    Vale, Juliana A.; Faustino, Wagner M., E-mail: julianadqf@yahoo.com.br [Departamento de Quimica, Universidade Federal da Paraiba, Joao Pessoa, PB (Brazil); Zampieri, Davila de S.; Moran, Paulo J.S.; Rodrigues, Jose A.R. [Instituto de Quimica, Universidade Estadual de Campinas, SP (Brazil); Sa, Gilberto F. de [Departamento de Quimica Fundamental, CCEN, Universidade Federal de Pernambuco, Recife, PE (Brazil)

    2012-08-15

    In this work we report the use of lanthanide nitrates [Ln(NO{sub 3}){sub 3}] acting as catalyst in direct one pot synthesis of 3-benzoyl- and 3-acetyl-1,2,4-oxadiazoles derivatives from ketones, nitriles and nitric acid. This is the first example of one-pot synthesis of benzoyl- and acetyl 1,2,4-oxadiazoles derivatives preparation using acetophenones derivates with electron-donator groups. (author)

  1. Analysis of benzoic and cinnamic acid derivatives of some medicinal plants in Serbia

    Directory of Open Access Journals (Sweden)

    Đurđević L.

    2013-01-01

    Full Text Available Natural phenolics, which are ubiquitously distributed in plants, have been reported as functional factors in phytotherapy. We have examined phenolic compounds in the leaves and inflorescences of five significant medicinal plants of different plant families: Salvia officinalis (Lamiaceae; Achillea clypeolata (Asteraceae; Nymphaea alba (Nymphaeaceae; Rumex acetosella (Polygonaceae and Allium ursinum (Alliaceae. The examined species were rich in total phenolics (up to 30.88 mg/g dry weight. According to their total phenolics contents, the plants can be arranged in the following order: A. clypeolata>N. alba>S. officinalis>R. acetosella>A. ursinum. Free phenolics prevailed in all species in comparison to the bound forms (63.72-82.68% of total phenolics. The highest content of total free phenolics was measured in the tissues of A. clypeolata and N. alba, and the lowest in A. ursinum. Five phenolic acids were isolated and measured. p-Coumaric and ferulic acids as derivatives of cinnamic acid prevailed in the leaves of R. acetosella and A. ursinum (up to 4.81%. [Projekat Ministarstva nauke Republike Srbije, br. 173018

  2. DFT computational study on decarboxylation mechanism of salicylic acid and its derivatives in the anionic state

    Science.gov (United States)

    Gao, Lu; Hu, Yanying; Zhang, Huitu; Liu, Yanchun; Song, Zhidan; Dai, Yujie

    2016-07-01

    The mechanisms of the decarboxylation of salicylic acid anion and its ortho substituted derivatives in gas phase and aqueous solution have been investigated by B3LYP method of DFT theory using the 6-31++G (d,p) basis set. The decarboxylation process includes hydrogen transfers from hydroxyl to carboxyl group and from carboxyl to the α-C of the aryl ring. The mechanism suggested is a pseudo-unimolecular decomposition of the salicylic acid anion and the hydrogen transfer from carboxyl to the α-C of the aryl ring is the rate determining step. Compared with the decarboxylation process in gas phase, the energy barriers in aqueous solution approximately declined by 25%-31%with the water mediation of the hydrogen transfer from carboxyl to the α-C of the aryl ring. The effects of substituents at the ortho position on the decarboxylation process were also investigated. Both the electron donating CH3 and withdrawing group NO2 at the ortho position of carboxyl group can further reduce the reaction energy barriers of the decarboxylation of salicylic acid anions.

  3. 取代苯甲酸类化合物在正辛醇中的固液平衡%Solid-Liquid Equilibria of Benzoic Acid Derivatives in 1-Octanol

    Institute of Scientific and Technical Information of China (English)

    贾青竹; 马沛生; 马少娜; 王昶

    2007-01-01

    The solid-liquid equilibrium of benzoic acid derivatives in 1-octanol was first determined in this article.Using a laser monitoring observation technique, the solubility data of o-amino-benzoic acid, p-amino-benzoic acid,o-chloro-benzoic acid, and m-nitro-benzoic acid in 1-octanol were measured by the polythermal method in the temperature range of 20-50 ℃. The experimental data were regressed with the Wilson equation and the λH equation. The experimental results showed that the solubility of the four chemicals in 1-octanol increased significantly with temperature. The results indicate that the molecular structure and interactions affect the solubility significantly.The solubility order of the benzoic acid derivatives is as follows: m-nitro-benzoic acid>o-chloro-benzoic acid>o-amino-benzoic acid>p-amino-benzoic acid. Both the Wilson equation and λH equation are in good agreement with the experimental data.

  4. Two pyrazine derivatives as inhibitors of the cold rolled steel corrosion in hydrochloric acid solution

    Energy Technology Data Exchange (ETDEWEB)

    Deng Shuduan, E-mail: dengshuduan@163.co [Faculty of Wood Science and Decoration Technology, Southwest Forestry University, Kunming 650224 (China); Li Xianghong; Fu Hui [Department of Fundamental Courses, Southwest Forestry University, Kunming 650224 (China)

    2011-02-15

    Research highlights: Two pyrazine derivatives of 2-aminopyrazine (AP) and 2-amino-5-bromopyrazine (ABP) are good inhibitors for the corrosion of steel in 1.0 M HCl solution. The inhibition efficiency follows the order: ABP > AP. The substitution Br of ABP is the additional centre of adsorption and increases the electron density of pyrazine ring, which can facilitate its adsorption on the metal surface. For either ABP or AP, the adsorption obeys Langmuir adsorption isotherm. Both ABP and AP act as mixed-type inhibitors. - Abstract: The inhibition effect of two pyrazine derivatives of 2-aminopyrazine (AP) and 2-amino-5-bromopyrazine (ABP) on the corrosion of cold rolled steel (CRS) in 1.0 M hydrochloric acid (HCl) was studied by weight loss, potentiodynamic polarization curves, and electrochemical impedance spectroscopy (EIS) methods. The results show that both AP and ABP are good inhibitors, and inhibition efficiency follows the order: ABP > AP. The adsorption of each inhibitor on CRS surface obeys Langmuir adsorption isotherm. Potentiodynamic polarization curves show that two pyrazine derivatives act as mixed-type inhibitors. EIS spectra exhibit one capacitive loop and confirm the inhibitive ability.

  5. Synthesis and Insecticidal Activity of Novel Camptothecin Derivatives Containing Analogs of Chrysanthemic Acid Moieties

    Institute of Scientific and Technical Information of China (English)

    DENG Li; ZHANG Lan; CAO Li-dong; XIE Ru-liang; ZHANG Yan-ning; HE Wei-zhi; JIANG Hong-yun

    2014-01-01

    Creating high-efifcient and environment-friendly pesticides is very important to produce the pollution free agriculture food and maintain the balance of the survival environmental of the human being. According to reports, camptothecin (CPT) and its derivatives are now being explored as a class of botanical insecticide in agriculture due to its novel mode of action. In order to improve the insecticidal activity of CPT, ten novel camptothecin (1) and 10-hydroxycamptothecin (2) derivatives (1a, 1b, 1c, 1d, 1e;2a, 2b, 2c, 2d, 2e) were designed and synthesized via esteriifcation with analogs of chrysanthemic acid, which have outstanding insecticidal activity. The results showed that compound 2a exhibited potent antifeeding effect and the best contact toxicity among the target compounds against the third-instar larvae of beet armyworm, Spodoptera exigua Hübner. Compound 2a was also found to be the most effective cytotoxic compound to the tested insect cell lines, IOZCAS-Spex-II, which were established from the fat bodies of S. exigua. It was proposed that the 10-hydroxyl group in the camptothecin derivatives is a key factor for the antifeeding activity of a compound. The nature of the substituents was considered the major factor in determining the insecticidal activity of these compounds.

  6. Changes of reanalysis-derived Northern Hemisphere summer warm extreme indices during 1948-2006 and links with climate variability

    Science.gov (United States)

    Fang, Xingqin; Wang, Anyu; Fong, Soi-kun; Lin, Wenshi; Liu, Ji

    2008-08-01

    those on NH-water. TX90P increases more rapidly than TN90P and significant upward (downward) trends in TX90P have more (less) areal coverage than significant upward (downward) trends in TN90P on NH-land during 1948-2006. ENSO mainly modulates interannual variations, especially during PDO warm phase after the 1980s, and it has opposite impacts in Indian Ocean, South China Sea, south and southeast Asia coasts and in the interior Asia. PDO mainly controls the long-term significant upward trend in the central tropical Atlantic and downward trend in Mongolia and north China. NAO indices of different seasons have different impacted locations, the most obvious positive trend reversion in the late 1970s in south Greenland offshore is related to the interdecadal variation of summer NAO. An abrupt shift of NH summer diurnal temperature range in NCEP reanalysis data in 1967 suggests that the derived results related to the very high minimum temperature on NH-land before 1967 be accepted with care.

  7. 2-Cyanoethylmercapturic acid (CEMA) in the urine as a possible indicator of exposure to acrylonitrile.

    Science.gov (United States)

    Jakubowski, M; Linhart, I; Pielas, G; Kopecký, J

    1987-12-01

    The aim of this study was to evaluate the efficiency of metabolism of acrylonitrile (ACN) to N-acetyl-S-(2-cyanoethyl)-L-cysteine (2-cyanoethylmercapturic acid (CEMA) in man, the kinetics of excretion of this metabolite, and the relation between the uptake of ACN and the excretion of CEMA in urine. Eleven experiments were performed on six male volunteers exposed for eight hours to ACN at concentrations of 5 or 10 mg/m3. The average respiratory retention of ACN was 52% and 21.8% of the retained ACN was excreted as CEMA in urine. Elimination approximated first order kinetics with half life of about eight hours. The best correlation between the uptake of ACN in the lungs and excretion of CEMA in urine was obtained when the concentration of CEMA in the urine fraction, collected between the sixth and eighth hours after the beginning of exposure, was adjusted to a specific gravity of 1.016 (y = 0.33x-13.3; r = 0.83). CEMA excretion, however, cannot be used as an individual index of exposure.

  8. Isolation and Characterization of Acid-Tolerant, Thermophilic Bacteria for Effective Fermentation of Biomass-Derived Sugars to Lactic Acid

    Science.gov (United States)

    Patel, Milind A.; Ou, Mark S.; Harbrucker, Roberta; Aldrich, Henry C.; Buszko, Marian L.; Ingram, Lonnie O.; Shanmugam, K. T.

    2006-01-01

    Biomass-derived sugars, such as glucose, xylose, and other minor sugars, can be readily fermented to fuel ethanol and commodity chemicals by the appropriate microbes. Due to the differences in the optimum conditions for the activity of the fungal cellulases that are required for depolymerization of cellulose to fermentable sugars and the growth and fermentation characteristics of the current industrial microbes, simultaneous saccharification and fermentation (SSF) of cellulose is envisioned at conditions that are not optimal for the fungal cellulase activity, leading to a higher-than-required cost of cellulase in SSF. We have isolated bacterial strains that grew and fermented both glucose and xylose, major components of cellulose and hemicellulose, respectively, to l(+)-lactic acid at 50°C and pH 5.0, conditions that are also optimal for fungal cellulase activity. Xylose was metabolized by these new isolates through the pentose-phosphate pathway. As expected for the metabolism of xylose by the pentose-phosphate pathway, [13C]lactate accounted for more than 90% of the total 13C-labeled products from [13C]xylose. Based on fatty acid profile and 16S rRNA sequence, these isolates cluster with Bacillus coagulans, although the B. coagulans type strain, ATCC 7050, failed to utilize xylose as a carbon source. These new B. coagulans isolates have the potential to reduce the cost of SSF by minimizing the amount of fungal cellulases, a significant cost component in the use of biomass as a renewable resource, for the production of fuels and chemicals. PMID:16672461

  9. Harnessing Yeast Peroxisomes for Biosynthesis of Fatty-Acid-Derived Biofuels and Chemicals with Relieved Side-Pathway Competition

    DEFF Research Database (Denmark)

    Zhou, Yongjin J.; Buijs, Nicolaas A; Zhu, Zhiwei

    2016-01-01

    to peroxisomes can increase the production of fatty-acid-derived fatty alcohols, alkanes and olefins up to 700%. In addition, we demonstrate that biosynthesis of these chemicals in the peroxisomes results in significantly decreased accumulation of byproducts formed by competing enzymes. We further demonstrate...... environment for biosynthesis. Peroxisomes are cellular organelles where fatty acids are degraded, a process that is inhibited under typical fermentation conditions making them an interesting workhouse for production of fatty-acid-derived molecules. Here, we show that targeting synthetic pathways...

  10. New Chiral Calixarene Derivatives: Syntheses and Their Chiral Recognition Toward Amino Acids by UV-Vis Spectroscopy

    Institute of Scientific and Technical Information of China (English)

    2008-01-01

    Three novel types of chiral calixarene derivatives 5, 8, and 10 were designed and synthesized by introducing chiral units to parent calixarenes. Their chiralities were confirmed by rotational analysis. Chiral recognition properties of these host compounds towards L- and D-threonine were studied by UV-Vis spectroscopy. The results indicated that calixarene derivatives 5 and 8 exhibited good chiral recognition capabilities toward L- or D-threonine. Although calixarene derivative 10 had no evident chiral recognition ability, the supramolecules of calixarene derivative 10 with L- or D-threonine showed a hypochromic effect or hyperchromic effect respectively. Therefore, calixarene derivative 10 might serve as a good chiral UV-indicator.

  11. Removal of free fatty acid in Palm Fatty Acid Distillate using sulfonated carbon catalyst derived from biomass wastefor biodiesel production

    Science.gov (United States)

    Hidayat, Arif; Rochmadi; Wijaya, Karna; Budiman, Arief

    2016-01-01

    In this research, the esterification of PFAD using the sulfonatedcoconut shell biochar catalyst was studied. Carbon solid catalysts were prepared by a sulfonation of carbonized coconut shells. The performances of the catalysts were evaluated in terms of the reaction temperatures, the molar ratios of methanol to PFAD, the catalyst loading and the reaction times. The reusability of the solid acid carbon catalysts was also studied in this work. The results indicated that the FFA conversion was significantly increased with increasing catalyst loading and reaction times. It can be concluded that the optimal conditions were an PFAD to methanol molar ratio of 1:12, the amount of catalyst of 10%w, and reaction temperature of 60oC.At this optimum condition, the conversion to biodieselreached 88%.

  12. Effect of a phytogenic additive on blood serum indicator levels and fatty acids profile in fattening turkeys meat

    Directory of Open Access Journals (Sweden)

    Branislav Gálik

    2015-12-01

    Full Text Available The aim of the study was to determine the effect of a phytogenic additive on blood serum indicator levels and fatty acids profile of breast, leg muscles and liver in fattening turkeys. The experiment was realized in private turkey farm and in the Department of Animal Nutrition, Faculty of Agrobiology and Food Resources, Slovak University of Agriculture in Nitra. A total of 300 clinically healthy female turkeys (broad-breasted white turkey, hybrid XL were used in the experiment. Female turkeys were randomly divided into two groups (150 pcs per each. In the control group, turkey were fed with standard complete feed mixtures for fattening, in the experimental group, standard diets from the beginning to 12th week were supplemented with the a blend of essential oils from origanum, anise and citrus fruits as well as a prebiotic rich fructooligosaccharides in dosage 1kg per 1000 kg of feed mixture. Fattening lasted 18 weeks. Blood serum was collected at the end of the experiment, during the slaughter of birds. Samples of breast and leg muscles, and liver for fatty acids composition evaluation were collected during birds dissection (10 samples per each group. After the 12 weeks of phytoadditive supplementation, a tendency of lower activity of serum alanine aminotransferase (53.963 vs. 3.499 U/L and aspartate aminotransferase (6.238 vs. 1.012 U/L in experimental group of turkeys was found (P0.01 content of cis-8,11,14-eicosadienoic and arachidonic acids. The phytoadditive supplementation significantly (P<0.01 decreased content of some unsaturated fatty acids in turkeys tissues, as well. In experimental group of turkey have been recorded lower level of elaidic and oleic acids in the breast muscle and cis-11,14-eicosadienoic and arachidonic acids in the liver, compare to birds from control group.

  13. Design, synthesis and biological evaluation of novel L-ascorbic acid-conjugated pentacyclic triterpene derivatives as potential influenza virus entry inhibitors.

    Science.gov (United States)

    Wang, Han; Xu, Renyang; Shi, Yongying; Si, Longlong; Jiao, Pingxuan; Fan, Zibo; Han, Xu; Wu, Xingyu; Zhou, Xiaoshu; Yu, Fei; Zhang, Yongmin; Zhang, Liangren; Zhang, Lihe; Zhou, Demin; Xiao, Sulong

    2016-03-03

    Since the influenza viruses can rapidly evolve, it is urgently required to develop novel anti-influenza agents possessing a novel mechanism of action. In our previous study, two pentacyclic triterpene derivatives (Q8 and Y3) have been found to have anti-influenza virus entry activities. Keeping the potential synergy of biological activity of pentacyclic triterpenes and l-ascorbic acid in mind, we synthesized a series of novel l-ascorbic acid-conjugated pentacyclic triterpene derivatives (18-26, 29-31, 35-40 and 42-43). Moreover, we evaluated these novel compounds for their anti-influenza activities against A/WSN/33 virus in MDCK cells. Among all evaluated compounds, the 2,3-O,O-dibenzyl-6-deoxy-l-ascorbic acid-betulinic acid conjugate (30) showed the most significant anti-influenza activity with an EC50 of 8.7 μM, and no cytotoxic effects on MDCK cells were observed. Time-of-addition assay indicated that compound 30 acted at an early stage of the influenza life cycle. Further analyses revealed that influenza virus-induced hemagglutination of chicken red blood cells was inhibited by treatment of compound 30, and the interaction between the influenza hemagglutinin (HA) and compound 30 was determined by surface plasmon resonance (SPR) with a dissociation constant of KD = 3.76 μM. Finally, silico docking studies indicated that compound 30 and its derivative 31 were able to occupy the binding pocket of HA for sialic acid receptor. Collectively, these results suggested that l-ascorbic acid-conjugated pentacyclic triterpenes were promising anti-influenza entry inhibitors, and HA protein associated with viral entry was a promising drug target.

  14. Gallic acid-based indanone derivative interacts synergistically with tetracycline by inhibiting efflux pump in multidrug resistant E. coli.

    Science.gov (United States)

    Dwivedi, Gaurav Raj; Tiwari, Nimisha; Singh, Aastha; Kumar, Akhil; Roy, Sudeep; Negi, Arvind Singh; Pal, Anirban; Chanda, Debabrata; Sharma, Ashok; Darokar, Mahendra P

    2016-03-01

    The purpose of the present study was to study the synergy potential of gallic acid-based derivatives in combination with conventional antibiotics using multidrug resistant cultures of Escherichia coli. Gallic acid-based derivatives significantly reduced the MIC of tetracycline against multidrug resistant clinical isolate of E. coli. The best representative, 3-(3',4,'5'-trimethoxyphenyl)-4,5,6-trimethoxyindanone-1, an indanone derivative of gallic acid, was observed to inhibit ethidium bromide efflux and ATPase which was also supported by in silico docking. This derivative extended the post-antibiotic effect and decreased the mutation prevention concentration of tetracycline. This derivative in combination with TET was able to reduce the concentration of TNFα up to 18-fold in Swiss albino mice. This derivative was nontoxic and well tolerated up to 300 mg/kg dose in subacute oral toxicity study in mice. This is the first report of gallic acid-based indanone derivative as drug resistance reversal agent acting through ATP-dependent efflux pump inhibition.

  15. Radioiodinated phenylalkyl malonic acid derivatives as pH-sensitive SPECT tracers.

    Directory of Open Access Journals (Sweden)

    Matthias Bauwens

    Full Text Available INTRODUCTION: In vivo pH imaging has been a field of interest for molecular imaging for many years. This is especially important for determining tumor acidity, an important driving force of tumor invasion and metastasis formation, but also in the process of apoptosis. METHODS: 2-(4-[(123I]iodophenethyl-2-methylmalonic acid (IPMM, 2-(4-[(123I]iodophenethyl-malonic acid (IPM, 2-(4-[(123I]iodobenzyl-malonic acid (IBMM and 4-[(123I]iodophthalic acid (IP were radiolabeled via the Cu(+ isotopic nucleophilic exchange method. All tracers were tested in vitro in buffer systems to assess pH driven cell uptake. In vivo biodistribution of [(123I]IPMM and [(123I]IPM was determined in healthy mice and the pH targeting efficacy in vivo of [(123I]IPM was evaluated in an anti-Fas monoclonal antibody (mAb apoptosis model. In addition a mouse RIF-1 tumor model was explored in which tumor pH was decreased from 7.0 to 6.5 by means of induction of hyperglycemia in combination with administration of meta-iodobenzylguanidine. RESULTS: Radiosynthesis resulted in 15-20% for iodo-bromo exchange and 50-60% yield for iodo-iodo exchange while in vitro experiments showed a pH-sensitive uptake for all tracers. Shelf-life stability and in vivo stability was excellent for all tracers. [(123I]IPMM and [(123I]IPM showed a moderately fast predominantly biliary clearance while a high retention was observed in blood. The biodistribution profile of [(123I]IPM was found to be most favorable in view of pH-specific imaging. [(123I]IPM showed a clear pH-related uptake pattern in the RIF-1 tumor model. CONCLUSION: Iodine-123 labeled malonic acid derivates such as [(123I]IPM show a clearly pH dependent uptake in tumor cells both in vitro and in vivo which allows to visualize regional acidosis. However, these compounds are not suitable for detection of apoptosis due to a poor acidosis effect.

  16. Effects of salvianolic acid B on proliferation, neurite outgrowth and differentiation of neural stem cells derived from the cerebral cortex of embryonic mice

    Institute of Scientific and Technical Information of China (English)

    2010-01-01

    Salvianolic acid B is isolated from Salvia miltiorrhiza,the root of which is widely used as a traditional Chinese medicine to treat stroke.However,little is known about how salvianolic acid B influences growth characteristics of neural stem cells (NSCs).The purpose of the present study was to evaluate the effects of salvianolic acid B on proliferation,neurite outgrowth and differentiation of NSCs derived from the cerebral cortex of embryonic mice using MTT,flow cytometry,immunofluorescence and RT-PCR.It was found that 20 μg mL·1 and 40 μg mL·1 salvianolic acid B had similar effects on proliferation of NSCs,and a suitable concentration of salvianolic acid B increased the number of NSCs and their derivative neurospheres.The growth-promoting activity of salvianolic acid B was dependent on and associated with an accumulation in the G2/S-phase cell population.Salvianolic acid B also promoted the neurite outgrowth of NSCs and their differentiation into neurons.The mRNA for tau,GFAP and nestin were present in differentiating neurospheres induced by salvianolic acid B.However,high-level expression of tau mRNA and low-level expression of GFAP mRNA was detected in differentiated cells,in contrast to the control conditions.This collective evidence indicates that exogenous salvianolic acid B is capable of promoting proliferation of neurospheres and differentiation towards the neuronal lineage in vitro and may act in the proliferation of NSCs and may promote NSC differentiation into neuronal cells.

  17. Chemical Architecture and Applications of Nucleic Acid Derivatives Containing 1,2,3-Triazole Functionalities Synthesized via Click Chemistry

    Directory of Open Access Journals (Sweden)

    Wei Gong

    2012-10-01

    Full Text Available There is considerable attention directed at chemically modifying nucleic acids with robust functional groups in order to alter their properties. Since the breakthrough of copper-assisted azide-alkyne cycloadditions (CuAAC, there have been several reports describing the synthesis and properties of novel triazole-modified nucleic acid derivatives for potential downstream DNA- and RNA-based applications. This review will focus on highlighting representative novel nucleic acid molecular structures that have been synthesized via the “click” azide-alkyne cycloaddition. Many of these derivatives show compatibility for various applications that involve enzymatic transformation, nucleic acid hybridization, molecular tagging and purification, and gene silencing. The details of these applications are discussed. In conclusion, the future of nucleic acid analogues functionalized with triazoles is promising.

  18. In Vivo Anti-inflammatory Activity of Lipoic Acid Derivatives in Mice 

    Directory of Open Access Journals (Sweden)

    Brunon Kwiecień

    2013-04-01

    Full Text Available Background: In mammals lipoic acid (LA and its reduced form dihydrolipoic acid (DHLA function as cofactors for multienzymatic complexes catalyzing the decarboxylation of α-ketoacids. Moreover, LA is used as a drug in a variety of diseases including inflammatory diseases. The aim of the study was to examine anti-inflammatory properties of LA metabolites.Material/methods:The present paper reports the chemical synthesis of 2,4-bismethylthio-butanoic acid (BMTBA and tetranor-dihydrolipoic acid (tetranor-DHLA. BMTBA is one of the biotransformation products of LA, while tetranor-DHLA is an analogue of DHLA. Structural identity of these compounds was confirmed by 1H NMR. These compounds were assessed for their anti-inflammatory activity in mice. For this purpose, the zymosan-induced peritonitis and the carrageenan-induced hind paw edema animal models were applied.Results/conclusions: The obtained results indicated that the early vascular permeability measured at 30 min of zymosan-induced peritonitis was significantly inhibited in groups receiving BMTBA (10, 30, 50 mg/kg. The early infiltration of neutrophils measured at 4 hours of zymosan-induced peritonitis was inhibited in the group receiving BMTBA (50 mg/kg and tetranor-DHLA (50 mg/kg. The results indicated that the increase in paw edema was significantly inhibited in the groups receiving BMTBA (50, 100 mg/kg and tetranor-DHLA (30, 50 mg/kg. In summary, the present studies clearly demonstrated that both BMTBA and tetranor-DHLA were able to act as anti-inflammatory agents. This is the first study examining in vivo the anti-inflammatory properties of LA metabolites.

  19. Hydrazino-methoxy-1,3,5-triazine Derivatives' Excellent Corrosion Organic Inhibitors of Steel in Acidic Chloride Solution.

    Science.gov (United States)

    El-Faham, Ayman; Osman, Sameh M; Al-Lohedan, Hamad A; El-Mahdy, Gamal A

    2016-06-01

    The corrosion inhibition performance of 2-hydrazino-4,6-dimethoxy-1,3,5-tirazine (DMeHT), 2,4-dihydrazino-6-methoxy-1,3,5-triaizine (DHMeT), and 2,4,6-tridydrazino-1,3,5-triaizne (TH₃) on steel corrosion in acidic media was examined using electrochemical techniques. The results showed 2,4-Ddihydrazino-6-methoxy-1,3,5-triaizine (DHMeT) gave the best corrosion protection performance among the other hydrazino derivatives even at a low concentration of 25 ppm (95%). The number of hydrazino groups play an important role in the corrosion inhibition, where the two hydrazine groups increased the electrostatic interactions between the protonated tested compounds, the negatively charged steel surface resulted from the adsorption of the chloride anions, and the presence of the methoxy group made the compound more reliable for formation of film protection on the surface of steel through the lone pair of oxygen atoms. Electrochemical Impedance Spectroscopy (EIS) measurements suggested that the corrosion process of steel in presence of the hydrazino-s-triazine derivatives (TH₃, DMeHT and DHMeT) were being controlled by the charge transfer reaction. Polarization curves indicated that the examined TH₃, DMeHT and DHMeT behaved as mixed type inhibitors.

  20. The Associations of Serum Uric Acid with Obesity-Related Acanthosis nigricans and Related Metabolic Indices

    Science.gov (United States)

    Rampersad, Sharvan; You, Hui; Sheng, Chunjun; Yang, Peng; Cheng, Xiaoyun; Bu, Le

    2017-01-01

    Objective. Recent studies have shown that hyperuricemia (HUA) is associated with hypertension, dyslipidemia, insulin resistance, and metabolic syndrome (MetS). We aimed to examine the relationship of serum UA with Acanthosis nigricans (AN) and related metabolic indices in obese patients. Methods. A cross-sectional study with 411 obese patients recruited from our department was analyzed in this study. Weight, body mass index (BMI), UA, lipid profile, liver function, and renal function were measured in all participants. Oral glucose tolerance tests were performed, and serum glucose, insulin, and C peptide were measured at 0, 30, 60, 120, and 180 min. Results. AN group had higher serum UA levels than OB group. Circulating UA levels were associated with BMI, dyslipidemia, hypertension, IR, and AN. In logistic regression analyses (multivariable‐adjusted), a high serum UA level was associated with high odds ratios (ORs) (95% confidence interval [CI]) for AN in females (ORs = 3.00 and 95% CI [1.02–8.84]) and males (ORs = 6.07 and 95% CI [2.16–17.06]) in the highest quartile (Q4) of serum UA. Conclusions. Serum UA levels were positively associated with multiple metabolic abnormalities including obesity, hypertension, hyperglycemia, hyperlipidemia, and AN and may be an important risk factor in the development of AN; further evidences in vitro and in vivo are needed to investigate the direct or indirect relationship.

  1. THE "CHEMICAL OXYGEN DEMAND / TOTAL VOLATILE ACIDS" RATIO AS AN ANAEROBIC TREATABILITY INDICATOR FOR LANDFILL LEACHATES

    Directory of Open Access Journals (Sweden)

    R. C. Contrera

    2015-03-01

    Full Text Available Abstract In some operational circumstances a fast evaluation of landfill leachate anaerobic treatability is necessary, and neither Biochemical Methane Potential nor BOD/COD ratio are fast enough. Looking for a fast indicator, this work evaluated the anaerobic treatability of landfill leachate from São Carlos-SP (Brazil in a pilot scale Anaerobic Sequence Batch Biofilm Reactor (AnSBBR. The experiment was conducted at ambient temperature in the landfill area. After the acclimation, at a second stage of operation, the AnSBBR presented efficiency above 70%, in terms of COD removal, utilizing landfill leachate without water dilution, with an inlet COD of about 11,000 mg.L-1, a TVA/COD ratio of approximately 0.6 and reaction time equal to 7 days. To evaluate the landfill leachate biodegradability variation over time, temporal profiles of concentration were performed in the AnSBBR. The landfill leachate anaerobic biodegradability was verified to have a direct and strong relationship to the TVA/COD ratio. For a TVA/CODTotal ratio lower than 0.20, the biodegradability was considered low, for ratios between 0.20 and 0.40 it was considered medium, and above 0.40 it was considered high.

  2. Lewis Acid Pairs for the Activation of Biomass-derived Oxygenates in Aqueous Media

    Energy Technology Data Exchange (ETDEWEB)

    Roman, Yuriy [Massachusetts Inst. of Technology (MIT), Cambridge, MA (United States)

    2015-09-14

    The objective of this project is to understand the mechanistic aspects behind the cooperative activation of oxygenates by catalytic pairs in aqueous media. Specifically, we will investigate how the reactivity of a solid Lewis acid can be modulated by pairing the active site with other catalytic sites at the molecular level, with the ultimate goal of enhancing activation of targeted functional groups. Although unusual catalytic properties have been attributed to the cooperative effects promoted by such catalytic pairs, virtually no studies exist detailing the use heterogeneous water-tolerant Lewis pairs. A main goal of this work is to devise rational pathways for the synthesis of porous heterogeneous catalysts featuring isolated Lewis pairs that are active in the transformation of biomass-derived oxygenates in the presence of bulk water. Achieving this technical goal will require closely linking advanced synthesis techniques; detailed kinetic and mechanistic investigations; strict thermodynamic arguments; and comprehensive characterization studies of both materials and reaction intermediates. For the last performance period (2014-2015), two technical aims were pursued: 1) C-C coupling using Lewis acid and base pairs in Lewis acidic zeolites. Tin-, zirconium-, and hafnium containing zeolites (e.g., Sn-, Zr-, and Hf-Beta) are versatile solid Lewis acids that selectively activate carbonyl functional groups. In this aim, we demonstrate that these zeolites catalyze the cross-aldol condensation of aromatic aldehydes with acetone under mild reaction conditions with near quantitative yields. NMR studies with isotopically labeled molecules confirm that acid-base pairs in the Si-O-M framework ensemble promote soft enolization through α-proton abstraction. The Lewis acidic zeolites maintain activity in the presence of water and, unlike traditional base catalysts, in acidic solutions. 2) One-pot synthesis of MWW zeolite nanosheets for activation of bulky substrates. Through

  3. Bioactive compounds derived from the yeast metabolism of aromatic amino acids during alcoholic fermentation.

    Science.gov (United States)

    Mas, Albert; Guillamon, Jose Manuel; Torija, Maria Jesus; Beltran, Gemma; Cerezo, Ana B; Troncoso, Ana M; Garcia-Parrilla, M Carmen

    2014-01-01

    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.

  4. Study of a Triazole Derivative as Corrosion Inhibitor for Mild Steel in Phosphoric Acid Solution

    Directory of Open Access Journals (Sweden)

    Lin Wang

    2012-01-01

    Full Text Available The corrosion inhibition by a triazole derivative (PAMT on mild steel in phosphoric acid (H3PO4 solution has been investigated by weight loss and polarization methods. The experimental results reveal that the compound has a significant inhibiting effect on the corrosion of steel in H3PO4 solution. It also shows good corrosion inhibition at higher concentration of H3PO4. Potentiodynamic polarization studies have shown that the compound acts as a mixed-type inhibitor retarding the anodic and cathodic corrosion reactions with predominant effect on the cathodic reaction. The values of inhibition efficiency obtained from weight loss and polarization measurements are in good agreement. The adsorption of this compound is found to obey the Langmuir adsorption isotherm. Some kinetic and thermodynamic parameters such as apparent activation energy, frequency factor, and adsorption free energy have been calculated and discussed.

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

    Science.gov (United States)

    Guillamon, Jose Manuel; Torija, Maria Jesus; Beltran, Gemma; Troncoso, Ana M.; Garcia-Parrilla, M. Carmen

    2014-01-01

    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. PMID:24895623

  6. Synthesis and in vitro antitumor activities of lupeol dicarboxylic acid monoester derivatives.

    Science.gov (United States)

    Li, Weijie; Hao, Jing; Xiao, Yeyu

    2013-12-01

    Ten lupeol dicarboxylic acid monoester derivatives as new potent antitumor agents were synthesized and evaluated for in vitro antitumor activities against A549, LAC, HepG2 and HeLa cell lines. Among them, compounds 1-5 showed excellent antitumor activities against all tested tumor cell lines and compounds 6-10 exhibited high activities against A549, HepG2 and HeLa cells, exceeded lupeol, lupanol and doxorubicin. Compound 2 displayed the highest potent antitumor activities with IC50 values of 5.78 μM against A549 cell, 2.38 μM against LAC cell, 6.14 μM against HepG2 cell and 0.00842 μM against HeLa cell.

  7. Synthesis of some novel D-glucuronic acid acetylated derivatives as potential anti-tumor agents.

    Science.gov (United States)

    El-Nezhawy, Ahmed O H; Adly, Frady G; Eweas, Ahmed F; Hanna, Atef G; El-Kholy, Yehya M; El-Sayed, Shahenaz H; El-Naggar, Tarek B A

    2011-10-01

    A structurally diverse series of Δ(4,5) -uronamide derivatives have been chemically synthesized starting from D-glucuronic acid itself by means of acetylation, activation, amide bond formation and base-catalyzed elimination protocols. Structure elucidation for all products along with optimization of the synthetic steps is described. The synthesized compounds were evaluated for their in-vitro anti-tumor activity against MCF-7, TK-10 and UACC-62 cell lines. The compounds 5, 11, 13, 15 and 16 were the most active against TK-10 cell line. On the other hand, the most active compounds against the MCF-7 cell line were 11 and 15. However, compounds 5, 7, 11, 13, 15 and 16 were the most active against the UACC-62 cell line.

  8. Fluorinated betulinic acid derivatives and evaluation of their anti-HIV activity.

    Science.gov (United States)

    Li, Jizhen; Goto, Masuo; Yang, Xiaoming; Morris-Natschke, Susan L; Huang, Li; Chen, Chin-Ho; Lee, Kuo-Hsiung

    2016-01-01

    Several fluorinated derivatives of the anti-HIV maturation agent bevirimat (1) were synthesized and evaluated for anti-HIV replication activity. The modified positions were the C-2, C-3, C-28, and C-30 positions, either directly on the betulinic acid (2) skeleton or in the attached side chains. Compound 18, which has a trifluoromethyl group added to C-30 of its isopropenyl group, exhibited similar potency to 1 against HIV-1NL4-3. In total, our current studies support our prior conclusion that C-30 allylic modification is unlikely to be a pharmacophore for anti-HIV activity, but could be a meaningful route to manipulate other properties of 2-related compounds.

  9. Poly-Acrylic Acid Derivatives as Diesel Flow Improver for Paraffin-Based Daqing Diesel

    Institute of Scientific and Technical Information of China (English)

    Cuiyu Jiang; Ming Xu; Xiaoli Xi; Panlun Qi; Hongyan Shang

    2006-01-01

    Since the diesel products from paraffin-based Daqing crude oil showed low sensitivity to certain commercial diesel pour point depressant (PPDs) that resulted from the high content of paraffin, certain poly-acrylic acid derivatives (PADE) with-COOR,-COOH,-CONHR, and -COO-NH3+R groups by molecular design on the mechanics of diesel; PPDs were synthesized and evaluated as cold flow improver for Daqing 0# diesel in this paper. The pure PADE was superior to the commercial PPDs and displayed a substantial ability of wax crystals dispersion. There was a synergistic effect among the PADE and T1804 and secondary amine. The synergism clearly improved the low temperature performance of Daqing diesel products and could reduce the cold filter plugging point of 0# diesel by 6-7 ℃.

  10. Amino Acid Derivatives as New Zinc Binding Groups for the Design of Selective Matrix Metalloproteinase Inhibitors

    Directory of Open Access Journals (Sweden)

    Mariateresa Giustiniano

    2013-01-01

    Full Text Available A number of matrix metalloproteinases (MMPs are important medicinal targets for conditions ranging from rheumatoid arthritis to cardiomyopathy, periodontal disease, liver cirrhosis, multiple sclerosis, and cancer invasion and metastasis, where they showed to have a dual role, inhibiting or promoting important processes involved in the pathology. MMPs contain a zinc (II ion in the protein active site. Small-molecule inhibitors of these metalloproteins are designed to bind directly to the active site metal ions. In an effort to devise new approaches to selective inhibitors, in this paper, we describe the synthesis and preliminary biological evaluation of amino acid derivatives as new zinc binding groups (ZBGs. The incorporation of selected metal-binding functions in more complex biphenyl sulfonamide moieties allowed the identification of one compound able to interact selectively with different MMP enzymatic isoforms.

  11. Eicosanoids Derived From Arachidonic Acid and Their Family Prostaglandins and Cyclooxygenase in Psychiatric Disorders.

    Science.gov (United States)

    Yui, Kunio; Imataka, George; Nakamura, Hiroyuki; Ohara, Naoki; Naito, Yukiko

    2015-01-01

    Arachidonic acid (AA)-derived lipid mediators are called eicosanoids. Eicosanoids have emerged as key regulators of a wide variety of physiological responses and pathological processes, and control important cellular processes. AA can be converted into biologically active compounds by metabolism by cyclooxygenases (COX). Beneficial effect of COX-2 inhibitor celecoxib add-on therapy has been reported in early stage of schizophrenia. Moreover, add-on treatment of celecoxib attenuated refractory depression and bipolar depression. Further, the COX/prostaglandin E pathway play an important role in synaptic plasticity and may be included in pathophysiology in autism spectrum disorders (ASD). In this regard, plasma transferrin, which is an iron mediator related to eicosanoid signaling, may be related to social impairment of ASD. COX-2 is typically induced by inflammatory stimuli in the majority of tissues, and the only isoform responsible for propagating the inflammatory response. Thus, COX-2 inhibitors considered as the best target for Alzheimer's disease.

  12. STRUCTURE BASED DRUG DESIGN STUDIES ON HETEROARYL PROPANOIC ACID DERIVATIVES AS PPARΓ AGONISTS

    Directory of Open Access Journals (Sweden)

    ARUN KUMAR,MANGA RATNAM,ARCHANA KUMARI, AJAY BABU

    2013-09-01

    Full Text Available Peroxisome proliferator-activated receptors (PPARs are a group of nuclear receptorproteins. Docking studies are based on several factors. Among 15 entries of PPARγ, 2Q6S wastaken for docking analysis, as it showed 418 most favored regions, 35 in additionally allowedregion and none of the residue in disallowed regions. To carry out drug designing, moleculeswere considered from the literature in which substitution of R1 position with dihydrofurylreported to have high dock score (-14.98 Kcal/mol than the remaining analogues, with bettergeometry and interactions. Hence docking analysis using heteroaryl propionic acid derivatives asanti-diabetic agents suggest the reproducibility of active molecules being predicted bycomputational docking studies using Auto dock software.

  13. Self-assembly into soft materials of molecules derived from naturallyoccurring fatty-acids

    Science.gov (United States)

    Zhang, Mohan

    The self-assembly of molecular gelators has provided an attractive route for the construction of nanostructured materials with desired functionalities. A well-defined paradigm for the design of molecular gels is needed, but none has yet been established. One of the important challenges to defining this paradigm is the creation of structure-property correlations for gelators at different distance scales. This dissertation centers on gaining additional insights in the relationship between small changes in gelator structures derived from long-chain, naturally-occurring fatty acids and the properties of the corresponding gels. This approach offers a reasonable method to probe the rational design of molecular gelators. (Abstract shortened by ProQuest.).

  14. Synthesis, characterization and physicochemical properties of oleic acid ether derivatives as biolubricant basestocks.

    Science.gov (United States)

    Salimon, Jumat; Salih, Nadia; Yousif, Emad

    2011-01-01

    Petroleum is a finite source as well as causing several environmental problems. Therefore petroleum needs to be replaced by alternative and sustainable sources. Plant oils and oleochemicals derived from them represent such alternative sources; the use of oleochemicals as biobased lubricants is of significant interest. This article presents a series of chemical modification on oleic acid to yield synthetic biolubricant basestocks. Measuring of density, volatility, cloud point (CP), pour point (PP), flash point (FP), viscosity index (VI), onset temperature (OT) and signal maximum temperature (SMT) was carried out for each compound. Furthermore, the friction and wear properties were measured using high-frequency reciprocating rig (HFRR). The results showed that octadecyl 9-octadecyloxy-10-hydroxyoctadecanoate exhibited the most favorable low-temperature performance (CP %ndash;26°C, PP %ndash;28°C) and the lowest ball wear scan diameter (42 µm) while propyl 9-propyloxy-10-hydroxyoctadecanoate exhibited the higher oxidation stability (OT 156°C).

  15. 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.

  16. Acid-base indicators in the venous and arterial blood of horses affected by recurrent airway obstruction (RAO).

    Science.gov (United States)

    Stopyra, A; Sobiech, P; Waclawska-Matyjasik, A

    2012-01-01

    The acid-base equilibrium is closely linked to gas exchange in the lungs, and respiratory exchange ratios are used to evaluate respiratory effectiveness and tissue oxygen levels. Acid-base indicators are determined in both arterial and venous blood samples. This study compares the usefulness of acid-base indicators of venous and arterial blood in monitoring the condition of horses with recurrent airway obstruction. Prior to treatment involving bronchodilating glucocorticoids, expectorant and mucolytic drugs, more pronounced changes were observed in venous blood (pH 7.283, pCO2 61.92 mmHg, pO2 35.541 mmHg, HCO3- 31.933 mmHg, BE 2.933 mmol/l, O2SAT 58.366%, ctCO2 38.333 mmol/l) than in arterial blood (pH 7.309, pCO2 53.478 mmHg, pO2 90.856 mmHg, HCO3- 28.50 mmHg, BE 3.133 mmol/l, O2SAT 93.375%, ctCO2 31.652 mmol/l), indicating compensated respiratory acidosis. The improvement of respiratory efficiency minimized acidosis symptoms in both venous blood (pH 7.365, pCO2 43.55 mmHg, pO2 47.80 mmHg, HCO3 30.325 mmHg, BE 3.050 mmol/l, O2SAT 80.10%, ctCO2 29.80 mmol/l) and arterial blood (pH 7.375, pCO2 39.268 mmHg, pO2 98.476 mmHg, HCO3- 26.651 mmHg, BE 4.956 mmol/l, O2SAT 98.475%, ctCO2 28.131 mmol/l). Venous blood parameters were marked by greater deviations from mean values, both before and after treatment. Acid-base indicators determined in venous blood are indicative of respiratory disturbances, but they do not support a comprehensive evaluation of gas exchange in the lungs.

  17. Tautomeric and Microscopic Protonation Equilibria of Anthranilic Acid and Its Derivatives.

    Science.gov (United States)

    Zapała, Lidia; Woźnicka, Elżbieta; Kalembkiewicz, Jan

    2014-01-01

    The acid-base chemistry of three zwitterionic compounds, namely anthranilic (2-aminobenzoic acid), N-methylanthranilic and N-phenylanthranilic acid has been characterized in terms of the macroconstants K a1, K a2, the isoelectric point pH I, the tautomerization constant K z and microconstants k 11, k 12, k 21, k 22. The potentiometric titration method was used to determine the macrodissociation constants. Due to the very poor water solubility of N-phenylanthranilic acid the dissociation constants pK a1 and pK a2 were determined in MDM-water mixtures [MDM is a co-solvent mixture, consisting of equal volumes of methanol (MeOH), dioxane and acetonitrile (MeCN)]. The Yasuda-Shedlovsky extrapolation procedure has been used to obtain the values of pK a1 and pK a2 in aqueous solutions. The pK a1 and pK a2 values obtained by this method are 2.86 ± 0.01 and 4.69 ± 0.03, respectively. The tautomerization constant K z describing the equilibrium between unionized form ⇌ zwitterionic form was evaluated by the K z method based on UV-VIS spectrometry. The method uses spectral differences between the zwitterionic form (found at isoelectric pH in aqueous solution) and the unionized form (formed in an organic solvent of low dielectric constant). The highest value of the K z constant has been observed in the case of N-methylantranilic acid (log10 K z = 1.31 ± 0.04). The values of log10 K z for anthranilic and N-phenylanthranilic acids are similar and have values of 0.93 ± 0.03 and 0.90 ± 0.05, respectively. The results indicate that the tested compounds, in aqueous solution around the isoelectric point pHI, occur mainly in the zwitterionic form. Moreover, the influence of the type of substituent and pH of the aqueous phase on the equilibrium were analyzed with regard to the formation and the coexistence of different forms of the acids in the examined systems.

  18. New Polyamides Based on Bis(p-amidobenzoic acid)-p-phenylene diacrylic acid and Hydantoin Derivatives: Synthesis and Characterization

    OpenAIRE

    FAGHIHI, Khalil

    2008-01-01

    Bis(p-amidobenzoic acid)-p-phenylene diacrylic acid (6) as a new monomer containing p-phenylenediacryloyl moiety was synthesized by using a 3-step reaction. At first p-phenylenediacrylic acid (3) was prepared by reaction of terephthal aldehyde (1) with malonic acid (2) in the presence of pyridine, and then diacid 3 was converted to p-phenylenediacryloyl chloride (4) by reaction with thionyl chloride. Finally bis(p-amidobenzoic acid)-p-phenylene diacrylic acid (6) was prepared by the ...

  19. N-Myristoylglutamic Acid Derivative of 3'-Fluoro-3'-Deoxythymidine as an Organogel.

    Science.gov (United States)

    Chhikara, Bhupender S; Tiwari, Rakesh; Parang, Keykavous

    2012-09-26

    Designing microbicidal gels of anti-HIV drugs for local application to prevent HIV infection is a subject of major interest. 3'-Fluoro-3'-deoxythymidine (FLT), a nucleoside reverse transcriptase inhibitor (NRTI), was conjugated with a N-myristoyl glutamate scaffold. The conjugate showed gelation at 1% (w/w) in different organic solvents, such as toluene, dichloromethane, and chloroform. The gels were opaque and stable at room temperature. The results indicate that myristoyl glutamate derivative of FLT can form an organogel. The gel could have potential application as a topical anti-HIV microbicidal agent.

  20. Inhibition effects of acetyl coumarines and thiazole derivatives on corrosion of zinc in acidic medium

    Indian Academy of Sciences (India)

    A V Shanbhag; T V Venkatesha; R A Prabhu; B M Praveen

    2011-06-01

    The corrosion inhibition characteristics of acetyl coumarine (AC), bromo acetyl coumarine (BAC) and thiazole derivatives (BTMQ and BTCQ) on the corrosion of zinc in 0.1 M HCl solution were investigated by weight loss, potentiodynamic polarization and impedance techniques. The inhibition efficiency increased with increase in inhibitor concentration upto 5 × 10-4 M, then gave almost same inhibition efficiency. The polarizationmeasurements indicated the mixed nature of inhibitors. The adsorption of compounds obeyed Langmuir’s adsorption isotherm. The thermodynamic functions for adsorption processes were evaluated.