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Sample records for agents mycophenolic acid

  1. Mycophenolic acid agents: is enteric coating the answer?

    Directory of Open Access Journals (Sweden)

    Manitpisitkul W

    2011-03-01

    Full Text Available Wana Manitpisitkul1, Sabrina Lee2, Matthew Cooper31Department of Pharmacy, University of Maryland Medical Center, Baltimore, MD, USA; 2Solid Organ Transplant Program, University of Utah Health Care, Salt Lake City, UT, USA; 3Department of Surgery, University of Maryland School of Medicine, Baltimore, MD, USAAbstract: Addition of mycophenolate mofetil (MMF to calcineurin-based immunosuppressive therapy has led to a significant improvement in graft survival and reduction of acute rejection in renal transplant recipients. However, in clinical practice, MMF dose reduction, interruption, or discontinuation due to hematological and gastrointestinal (GI side-effects occurred in up to 50% of the patients. Large retrospective analyses have demonstrated that patients requiring MMF dose manipulation due to adverse events experienced a higher rate of rejection and graft loss. Enteric-coated mycophenolate sodium (EC-MPS was developed with the goal of improving upper GI side-effects. Here, we review the efficacy and safety of EC-MPS in de novo kidney transplant recipient, and in stable renal transplant patients who were converted from MMF. The changes in GI-related adverse events using patient-reported outcome instruments are also reviewed.Keywords: enteric-coated mycophenolate sodium, mycophenolate mofetil, kidney transplant, efficacy, gastrointestinal tolerability

  2. Mycophenolic acid agents: is enteric coating the answer?

    OpenAIRE

    Manitpisitkul W; Lee S.; Cooper M

    2011-01-01

    Wana Manitpisitkul1, Sabrina Lee2, Matthew Cooper31Department of Pharmacy, University of Maryland Medical Center, Baltimore, MD, USA; 2Solid Organ Transplant Program, University of Utah Health Care, Salt Lake City, UT, USA; 3Department of Surgery, University of Maryland School of Medicine, Baltimore, MD, USAAbstract: Addition of mycophenolate mofetil (MMF) to calcineurin-based immunosuppressive therapy has led to a significant improvement in graft survival and reduction of acute rejection in ...

  3. Mycophenolate

    Science.gov (United States)

    ... doctor and pharmacist if you are allergic to aspartame or sorbitol. Ask your pharmacist for a list ... retardation), you should know that mycophenolate suspension contains aspartame, a source of phenylalanine.

  4. Mycophenolate

    Science.gov (United States)

    ... water. If you get the suspension in your eyes, rinse with plain water. Use wet paper towels to wipe up any spilled liquids.Mycophenolate helps prevent organ transplant rejection only as long as you are taking ...

  5. Mycophenolic acid formulations in adult renal transplantation – update on efficacy and tolerability

    Directory of Open Access Journals (Sweden)

    Déla Golshayan

    2009-04-01

    Full Text Available Déla Golshayan1,2, M Pascual2, Bruno Vogt11Service of Nephrology and Hypertension, 2Transplantation Centre and Transplantation Immunopathology Laboratory, Department of Medicine, Centre Hospitalier Universitaire Vaudois (CHUV, Lausanne University, 1011 Lausanne, SwitzerlandAbstract: The description more than 30 years ago of the role of de novo purine synthesis in T and B lymphocytes clonal proliferation opened the possibility for selective immunosuppression by targeting specific enzymatic pathways. Mycophenolic acid (MPA blocks the key enzyme inosine monophosphate dehydrogenase and the production of guanosine nucleotides required for DNA synthesis. Two MPA formulations are currently used in clinical transplantation as part of the maintenance immunosuppressive regimen. Mycophenolate mofetil (MMF was the first MPA agent to be approved for the prevention of acute rejection following renal transplantation, in combination with cyclosporine and steroids. Enteric-coated mycophenolate sodium (EC-MPS is an alternative MPA formulation available in clinical transplantation. In this review, we will discuss the clinical trials that have evaluated the efficacy and safety of MPA in adult kidney transplantation for the prevention of acute rejection and their use in new combination regimens aiming at minimizing calcineurin inhibitor toxicity and chronic allograft nephropathy. We will also discuss MPA pharmacokinetics and the rationale for therapeutic drug monitoring in optimizing the balance between efficacy and safety in individual patients.Keywords: kidney transplantation, immunosuppression, mycophenolic acid, mycophenolate mofetil, enteric-coated mycophenolate sodium, acute rejection, chronic allograft nephropathy

  6. Determination of mycophenolic acid and mycophenolate mofetil by high-performance liquid chromatography using postcolumn derivatization.

    Science.gov (United States)

    Renner, U D; Thiede, C; Bornhäuser, M; Ehninger, G; Thiede, H M

    2001-01-01

    An efficient method to lower the optical detection limit is described using the displacement of an absorption and emission band of an analyte after a polarity change in different solvents. This solvatochromic effect was used in a RP-HPLC assay for the fluorescence detection of mycophenolic acid (6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-5-phthalanyl)-4-methyl-4-hexenoic acid, MPA) and the prodrug mycophenolate mofetil (MMF), the N-(2-hydroxyethyl)morpholino ester of MPA. The rational to use fluorescence detection is based on the behavior of MMF and MPA, which fluoresce in a basic medium (pH >9.5). Following a simple protein precipitation, the analytes were separated in an isocratic RP-HPLC system. The postcolumn generation of the phenolate anions of MPA and MMF was achieved by addition of an aqueous sodium hydroxide solution regulated by a newly developed continuous-flow liquid control system. MPAG, not directly accessible for fluorescence detection, was analyzed after enzymatic deglucuronidation to MPA. Compared to published quantification limits for MPA and MMF by UV detection, this method is more than 100-fold more sensitive, with a lower limit of quantification of 45 fmol for both MPA and MMF. PMID:11195509

  7. Identification and Functional Analysis of the Mycophenolic Acid Gene Cluster of Penicillium roqueforti

    OpenAIRE

    Abdiel Del-Cid; Carlos Gil-Durán; Inmaculada Vaca; Juan F Rojas-Aedo; Ramón O García-Rico; Gloria Levicán; Renato Chávez

    2016-01-01

    The filamentous fungus Penicillium roqueforti is widely known as the ripening agent of blue-veined cheeses. Additionally, this fungus is able to produce several secondary metabolites, including the meroterpenoid compound mycophenolic acid (MPA). Cheeses ripened with P. roqueforti are usually contaminated with MPA. On the other hand, MPA is a commercially valuable immunosuppressant. However, to date the molecular basis of the production of MPA by P. roqueforti is still unknown. Using a bioinfo...

  8. Effects of sotrastaurin, mycophenolic acid and everolimus on human B-lymphocyte function and activation.

    Science.gov (United States)

    Matz, Mareen; Lehnert, Martin; Lorkowski, Christine; Fabritius, Katharina; Unterwalder, Nadine; Doueiri, Salim; Weber, Ulrike A; Mashreghi, Mir-Farzin; Neumayer, Hans-H; Budde, Klemens

    2012-10-01

    Humoral rejection processes may lead to allograft injury and subsequent dysfunction. Today, only one B-cell-specific agent is in clinical use and the effects of standard and new immunosuppressant substances on B-cell activation and function are not fully clarified. The impact of sotrastaurin, mycophenolic acid and everolimus on human B-lymphocyte function was assessed by analysing proliferation, apoptosis, CD80/CD86 expression and immunoglobulin and IL-10 production in primary stimulated B cells. In addition, B-cell co-cultures with pre-activated T cells were performed to evaluate the effect of the different immunosuppressive agents on T-cell-dependent immunoglobulin production. Sotrastaurin did not inhibit B-cell proliferation, CD80/CD86 expression, and IgG production and had only minor effects on IgM levels at the highest concentration administered. In contrast, mycophenolic acid and everolimus had strong effects on all B-cell functions in a dose-dependent manner. All immunosuppressive agents caused decreased immunoglobulin levels in T-cell-dependent B-cell cultures. The data provided here suggest that mycophenolic acid and everolimus, but not sotrastaurin, are potent inhibitors of human B-lymphocyte function and activation. PMID:22816666

  9. Time-dependent clearance of mycophenolic acid in renal transplant recipients

    NARCIS (Netherlands)

    R.M. van Hest (Reinier); T. van Gelder (Teun); R. Bouw (René); T. Goggin (Timothy); R. Gordon (Robert); R. Mamelok (Richard); R.A. Mathot (Ron)

    2007-01-01

    textabstractAims: Pharmacokinetic studies of the immunosuppressive compound mycophenolic acid (MPA) have shown a structural decrease in clearance (CL) over time after renal transplantation. The aim of this study was to characterize the time-dependent CL of MPA by means of a population pharmacokineti

  10. Simultaneous determination of ochratoxin A, mycophenolic acid and fumonisin B-2 in meat products

    DEFF Research Database (Denmark)

    Sørensen, Louise Marie; Mogensen, Jesper; Nielsen, Kristian Fog

    2010-01-01

    Here we present a method for simultaneous determination of the fungal metabolites mycophenolic acid, ochratoxin A (OTA) and fumonisin B-2 (FB2) in meat products. Extraction was performed with water-acetonitrile, followed by acetone-induced precipitation of salts and proteins. Purification and...

  11. Lab Scale Production of Mycophenolic Acid on Solid- phase Culture by Standard Strains of Penicillium Brevicompactum

    Directory of Open Access Journals (Sweden)

    M Afshari

    2012-05-01

    Full Text Available Introduction: Mycophenolic acid(MPA, a fungal mycotoxin, is produced by Penicillium brevicompactum and is used for the synthesis of immunosuppressive drugs in pharmaceutical industries. The present study was conducted to evaluate the possibility of mycophenolic acid(MPA production by standard strains of P. brevicompactum at laboratory level. Methods: Three strains of P. brevicompactum were provided from microbial culture collections. To stimulate MPA production, barley was used as culture medium, and dry heat, wet heat, and gamma radiation were used to sterilize the culture medium. Samples were taken from the culture medium at different intervals, and their MPA level was assessed by HPLC method. Results: P. brevicompactum strain which was prepared from Finland(VTT D-061157 was able to produce MPA more than two other strains(from Germany and Iran. The amount of MPA enhanced linearly until day 10, and after that became relatively constant. Gamma radiation was a suitable method to sterilize the substrate, and nylon bags were evaluated as an easy and cheap container for growing the fungus. Conclusion: Production of MPA with simple and cheap culture media to provide primary substance for immunosuppressive drugs such as mycophenolate mofetile and sodium mycophenolate would be possible.

  12. Identification and Functional Analysis of the Mycophenolic Acid Gene Cluster of Penicillium roqueforti.

    Directory of Open Access Journals (Sweden)

    Abdiel Del-Cid

    Full Text Available The filamentous fungus Penicillium roqueforti is widely known as the ripening agent of blue-veined cheeses. Additionally, this fungus is able to produce several secondary metabolites, including the meroterpenoid compound mycophenolic acid (MPA. Cheeses ripened with P. roqueforti are usually contaminated with MPA. On the other hand, MPA is a commercially valuable immunosuppressant. However, to date the molecular basis of the production of MPA by P. roqueforti is still unknown. Using a bioinformatic approach, we have identified a genomic region of approximately 24.4 kbp containing a seven-gene cluster that may be involved in the MPA biosynthesis in P. roqueforti. Gene silencing of each of these seven genes (named mpaA, mpaB, mpaC, mpaDE, mpaF, mpaG and mpaH resulted in dramatic reductions in MPA production, confirming that all of these genes are involved in the biosynthesis of the compound. Interestingly, the mpaF gene, originally described in P. brevicompactum as a MPA self-resistance gene, also exerts the same function in P. roqueforti, suggesting that this gene has a dual function in MPA metabolism. The knowledge of the biosynthetic pathway of MPA in P. roqueforti will be important for the future control of MPA contamination in cheeses and the improvement of MPA production for commercial purposes.

  13. Identification and Functional Analysis of the Mycophenolic Acid Gene Cluster of Penicillium roqueforti.

    Science.gov (United States)

    Del-Cid, Abdiel; Gil-Durán, Carlos; Vaca, Inmaculada; Rojas-Aedo, Juan F; García-Rico, Ramón O; Levicán, Gloria; Chávez, Renato

    2016-01-01

    The filamentous fungus Penicillium roqueforti is widely known as the ripening agent of blue-veined cheeses. Additionally, this fungus is able to produce several secondary metabolites, including the meroterpenoid compound mycophenolic acid (MPA). Cheeses ripened with P. roqueforti are usually contaminated with MPA. On the other hand, MPA is a commercially valuable immunosuppressant. However, to date the molecular basis of the production of MPA by P. roqueforti is still unknown. Using a bioinformatic approach, we have identified a genomic region of approximately 24.4 kbp containing a seven-gene cluster that may be involved in the MPA biosynthesis in P. roqueforti. Gene silencing of each of these seven genes (named mpaA, mpaB, mpaC, mpaDE, mpaF, mpaG and mpaH) resulted in dramatic reductions in MPA production, confirming that all of these genes are involved in the biosynthesis of the compound. Interestingly, the mpaF gene, originally described in P. brevicompactum as a MPA self-resistance gene, also exerts the same function in P. roqueforti, suggesting that this gene has a dual function in MPA metabolism. The knowledge of the biosynthetic pathway of MPA in P. roqueforti will be important for the future control of MPA contamination in cheeses and the improvement of MPA production for commercial purposes. PMID:26751579

  14. Mycophenolic acid inhibits replication of Type 2 Winnipeg, a cerebrospinal fluid-derived reovirus isolate

    OpenAIRE

    Hermann, Laura L.; Coombs, Kevin M.

    2004-01-01

    BACKGROUND: The role of reoviruses in human disease is uncertain. Most identified cases are sporadic and asymptomatic or produce minor upper respiratory or gastrointestinal symptoms. In November 1997, a reovirus was isolated from the cerebrospinal fluid of a severe combined immune deficient infant in Winnipeg, Manitoba. RNA characterization and sequencing studies demonstrated this reovirus isolate to be unique. Thus, the virus was named Type 2 Winnipeg (T2W).OBJECTIVES: Mycophenolic acid (MPA...

  15. PCR diagnosis of P. brevicompactum, a grape contaminant and mycophenolic acid producer.

    OpenAIRE

    Patiño, Belén; Medina, Angel; Mirian, Domenech; Mª Teresa, González-Jaén; Jiménez, Misericordia; Covadonga, Vázquez

    2007-01-01

    Abstract Penicillium brevicompactum is a ubiquitous fungal species that contaminates diverse substrates and commodities and produces an array of metabolites toxic to human and animals. In this work, we have obtained evidence, by LC-ion trap-mass spectrometry, of the ability of P. brevicompactum strains isolated from grapes to produce mycophenolic acid, a potent immunosuppressor. In order to facilitate early diagnosis of this species on commodities for human and animal consumption, ...

  16. Stability issues of mycophenolic acid in plasma: From patient to laboratory

    Directory of Open Access Journals (Sweden)

    Mathew B

    2009-01-01

    Full Text Available Although mycophenolate is widely prescribed in India, therapeutic drug monitoring of mycophenolic acid is not performed in most centers. This could be due to many factors such as the large investment and expertise required for high performance liquid chromatography, or the high costs involved as specialized refrigeration is required when transporting patient specimens to the laboratories with the facility to analyze MPA. The Clinical Pharmacology unit of the Christian Medical College Hospital routinely monitors the area under the curve of MPA. In order to determine if this unit could act as a central laboratory for MPA monitoring, the stability of MPA in plasma under a series of storage and transport conditions was assessed. The procedures involved the analysis of plasma specimens from patients on mycophenolate mofetil and blank plasma spiked with MPA reference standard. A range of low and high concentrations were separately analyzed to confirm long term and short term stability. The measured concentrations of MPA showed no significant change over 5 months when stored at -20° or over five days under conditions encountered during transport.

  17. Synthesis of PAMAM Dendrimers Loaded with Mycophenolic Acid to Be Studied as New Potential Immunosuppressants

    OpenAIRE

    Lorenzo Guazzelli; Felicia D’Andrea; Francesco Giorgelli; Giorgio Catelani; Alessandra Panattoni; Andrea Luvisi

    2015-01-01

    The terminal N-Boc protected diamino PAMAM 7 was condensed (EDC-DMAP) with two units of mycophenolic acid (MPA) giving the N-Boc protected dendron 8 in a good yield (76%). The ammonium trifluoroacetate 9 was prepared from 8 by acid treatment (TFA-THF-H2O) and was split into two equal parts. The first half was treated with di-2-pyridyl thionocarbonate (DPT) in the presence of Et3N to give the corresponding isothiocyanate 10. This was reacted with the second half of 9 providing the symmetrical ...

  18. Strain-Specific Synthesis of Mycophenolic Acid by Penicillium roqueforti in Blue-Veined Cheese

    OpenAIRE

    Engel, Günter; von Milczewski, Karl Ernst; Prokopek, Dieter; Teuber, Michael

    1982-01-01

    Twenty of 80 strains of Penicillium roqueforti were able to produce up to 600 mg of mycophenolic acid (MPA) liter−1 in 2% yeast extract-5% sucrose broth. Sixty-two of these strains had been isolated from the main blue-veined cheese varieties of western Europe or from starter cultures. Of these 62 dairy strains, only 7 had MPA-producing potential in vitro. These seven strains had all been isolated during the period 1975 to 1981 from the blue cheese of one individual factory. In cheese from the...

  19. Do cytostatic drugs reach drinking water? The case of mycophenolic acid.

    Science.gov (United States)

    Franquet-Griell, Helena; Ventura, Francesc; Boleda, M Rosa; Lacorte, Silvia

    2016-01-01

    Mycophenolic acid (MPA) has been identified as a new river contaminant according to its wide use and high predicted concentration. The aim of this study was to monitor the impact of MPA in a drinking water treatment plant (DWTP) that collects water downstream Llobregat River (NE Spain) in a highly densified urban area. During a one week survey MPA was recurrently detected in the DWTP intake (17-56.2 ng L(-1)). The presence of this compound in river water was associated to its widespread consumption (>2 tons in 2012 in Catalonia), high excretion rates and low degradability. The fate of MPA in waters at each treatment step of the DWTP was analyzed and complete removal was observed after pretreatment with chlorine dioxide. So far, MPA has not been described as water contaminant and its presence associated with its consumption in anticancer treatments is of relevance to highlight the importance of monitoring this compound. PMID:26552545

  20. Simultaneous determination of mycophenolate mofetil and its active metabolite, mycophenolic acid, by differential pulse voltammetry using multi-walled carbon nanotubes modified glassy carbon electrode

    International Nuclear Information System (INIS)

    A highly sensitive electrochemical sensor for the simultaneous determination of mycophenolate mofetil (MPM) and mycophenolic acid (MPA) was fabricated by multi-walled carbon nanotubes modified glassy carbon electrode (MWCNTs/GCE). The electrochemical behavior of these two drugs was studied at the modified electrode using cyclic voltammetry and adsorptive differential pulse voltammetry. MPM and MPA were oxidized at the GCE during an irreversible process. DPV analysis showed two oxidation peaks at 0.87 V and 1.1 V vs. Ag/AgCl for MPM and an oxidation peak at 0.87 V vs. Ag/AgCl for MPA in phosphate buffer solution of pH 5.0. The MWCNTs/GCE displayed excellent electrochemical activities toward oxidation of MPM and MPA relative to the bare GCE. The experimental design algorithm was used for optimization of DPV parameters. The electrode represents linear responses in the range 5.0 × 10−6 to 1.6 × 10−4 mol L−1 and 2.5 × 10−6 mol L−1 to 6.0 × 10−5 mol L−1 for MPM and MPA, respectively. The detection limit was found to be 9.0 × 10−7 mol L−1 and 4.0 × 10−7 mol L−1 for MPM and MPA, respectively. The modified electrode showed a good sensitivity and stability. It was successfully applied to the simultaneous determination of MPM and MPA in plasma and urine samples. - Highlights: • A new modified electrochemical sensor was constructed and used. • Multiwalled carbon nanotubes were used as the modifiers. • MPM and MPA were measured simultaneously at the low levels. • The sensor was used to the determination of MPA and MPM in real samples

  1. In Vitro Influence of Mycophenolic Acid on Selected Parameters of Stimulated Peripheral Canine Lymphocytes

    Science.gov (United States)

    Guzera, Maciej; Szulc-Dąbrowska, Lidia; Cywińska, Anna; Archer, Joy; Winnicka, Anna

    2016-01-01

    Mycophenolic acid (MPA) is an active metabolite of mycophenolate mofetil, a new immunosuppressive drug effective in the treatment of canine autoimmune diseases. The impact of MPA on immunity is ambiguous and its influence on the canine immune system is unknown. The aim of the study was to determine markers of changes in stimulated peripheral canine lymphocytes after treatment with MPA in vitro. Twenty nine healthy dogs were studied. Phenotypic and functional analysis of lymphocytes was performed on peripheral blood mononuclear cells cultured with mitogens and different MPA concentrations– 1 μM (10−3 mol/m3), 10 μM or 100 μM. Apoptotic cells were detected by Annexin V and 7-aminoactinomycin D (7-AAD). The expression of antigens (CD3, CD4, CD8, CD21, CD25, forkhead box P3 [FoxP3] and proliferating cell nuclear antigen [PCNA]) was assessed with monoclonal antibodies. The proliferation indices were analyzed in carboxyfluorescein diacetate succinimidyl ester (CFSE)-labeled cells. All analyses were performed using flow cytometry. The influence of MPA on apoptosis was dependent on the mechanism of cell activation and MPA concentration. MPA caused a decrease in the expression of lymphocyte surface antigens, CD3, CD8 and CD25. Its impact on the expression of CD4 and CD21 was negligible. Its negative influence on the expression of FoxP3 was dependent on cell stimulation. MPA inhibited lymphocyte proliferation. In conclusion, MPA inhibited the activity of stimulated canine lymphocytes by blocking lymphocyte activation and proliferation. The influence of MPA on the development of immune tolerance–expansion of Treg cells and lymphocyte apoptosis–was ambiguous and was dependent on the mechanism of cellular activation. The concentration that MPA reaches in the blood may lead to inhibition of the functions of the canine immune system. The applied panel of markers can be used for evaluation of the effects of immunosuppressive compounds in the dog. PMID:27138877

  2. Involvement of a Natural Fusion of a Cytochrome P450 and a Hydrolase in Mycophenolic Acid Biosynthesis

    OpenAIRE

    Hansen, Bjarne Gram; Mnich, Ewelina; Nielsen, Kristian Fog; Nielsen, Jakob Blæsbjerg; Nielsen, Morten Thrane; Mortensen, Uffe Hasbro; Larsen, Thomas Ostenfeld; Patil, Kiran Raosaheb

    2012-01-01

    Mycophenolic acid (MPA) is a fungal secondary metabolite and the active component in several immunosuppressive pharmaceuticals. The gene cluster coding for the MPA biosynthetic pathway has recently been discovered in Penicillium brevicompactum, demonstrating that the first step is catalyzed by MpaC, a polyketide synthase producing 5-methylorsellinic acid (5-MOA). However, the biochemical role of the enzymes encoded by the remaining genes in the MPA gene cluster is still unknown. Based on bioi...

  3. Development and validation of HPTLC method for quantification of mycophenolic acid

    Directory of Open Access Journals (Sweden)

    Shraddha Bhikaji Digole

    2014-08-01

    Full Text Available Normal 0 false false false EN-US X-NONE X-NONE MicrosoftInternetExplorer4 Mycophenolic Acid (MPA is an immunosuppressant; produced by Penicillium Sp.  In present study an analytical method is developed for analysis of MPA in fermentation broth by High Performance Thin Layer Chromatography (HPTLC, which has been a routine analytical technique by virtue of its advantages of low operating cost, high sample throughput and need for minimum sample clean-up. The method was carried out in TLC precoated silica gel on aluminium plate 60 F254. Various mobile phases were screened, out of which chloroform: methanol: water (9.2:0.7:0.1 gave the best separation at 220 nm by densitometric evaluation. The linearity was found to be in the range of 100-500ng with R2 value 0.997, % RSD of intraday and interday precision was found to be in the range of 1.22-2.03 and 1.23-2.81 respectively. Limit of Detection (LOD and Limit of Quantification (LOQ of mycophenolic acid was found to be 23.13ng/band and 77.09 ng/band respectively. Recovery of MPA obtained was found to be 98.76%; which suggest that the method is simple, accurate and reproducible. The experimental data was statistically analysed by Analysis of Variance (ANOVA which proves that, the developed chromatographic method can be used for routine analysis of MPA. /* Style Definitions */ table.MsoNormalTable {mso-style-name:"Table Normal"; mso-tstyle-rowband-size:0; mso-tstyle-colband-size:0; mso-style-noshow:yes; mso-style-priority:99; mso-style-qformat:yes; mso-style-parent:""; mso-padding-alt:0in 5.4pt 0in 5.4pt; mso-para-margin:0in; mso-para-margin-bottom:.0001pt; mso-pagination:widow-orphan; font-size:11.0pt; font-family:"Calibri","sans-serif"; mso-ascii-font-family:Calibri; mso-ascii-theme-font:minor-latin; mso-fareast-font-family:"Times New Roman"; mso-fareast-theme-font:minor-fareast; mso-hansi-font-family:Calibri; mso-hansi-theme-font:minor-latin; mso-bidi-font-family:"Times New Roman"; mso-bidi-theme-font:minor-bidi;}

  4. Strain-Specific Synthesis of Mycophenolic Acid by Penicillium roqueforti in Blue-Veined Cheese

    Science.gov (United States)

    Engel, Günter; von Milczewski, Karl Ernst; Prokopek, Dieter; Teuber, Michael

    1982-01-01

    Twenty of 80 strains of Penicillium roqueforti were able to produce up to 600 mg of mycophenolic acid (MPA) liter−1 in 2% yeast extract-5% sucrose broth. Sixty-two of these strains had been isolated from the main blue-veined cheese varieties of western Europe or from starter cultures. Of these 62 dairy strains, only 7 had MPA-producing potential in vitro. These seven strains had all been isolated during the period 1975 to 1981 from the blue cheese of one individual factory. In cheese from the market, MPA (up to 5 mg kg−1) was only found in samples of this same factory. With MPA-producing and -nonproducing strains for the experimental manufacture of blue cheese, MPA synthesis in cheese was only detected with strains which form MPA in yeast extract-sucrose broth. The maximum MPA level at 4 mg kg−1 was similar to that in commercial cheese. Toxicity of MPA was tested with two established human cell lines (Detroit 98 and Girardi Heart) and one established pig kidney cell line (AmII). PMID:16346004

  5. "Determination of mycophenolic acid in human plasma by high-performance liquid chromatography"

    Directory of Open Access Journals (Sweden)

    "Mehdi Ahadi Barzoki

    2005-05-01

    Full Text Available A simple, sensitive and reproducible HPLC method is presented for determination of mycophenolic acid(MPA in human plasma. Samples were prepared after precipitation of the plasma protein by addition of acetonitrile and naproxen was used as internal standard (I.S.. Separation was performed by reversedphase HPLC, using a Hamilton PRP-C18 Column, 51% acetonitrile and 49% potassium phosphate buffer (20 mM at pH 3.0 as mobile phase, flow rate of 1.0 ml/min, and UV detection at 215 nm. MPA and I.S. had retention times of 7.5 and 11.35 min, respectively. The method showed an acceptable linearity in the range of 0.1µg/ml-40µg/ml with r2 of .9992. The concentration of 0.1µg/ml was determined as quantification limit. Mean absolute recovery was 94.8%. The mean intra- and inter-day reproducibility of method was 4.6 and 11.4% respectively.

  6. Determination of mycophenolic acid in mest products using mixed mode reversed phase-anion exchange clean-up and liquid chromatography-high-resolution mass spectrometry

    DEFF Research Database (Denmark)

    Sørensen, Louise Marie; Nielsen, Kristian Fog; Jacobsen, Thomas;

    2008-01-01

    A method for determination of mycophenolic acid (MPA) in dry-cured ham, fermented sausage and liver pate is described. MPA was extracted from meat with bicarbonate-acetonitrile, further cleaned-up by mixed mode reversed phase-anion exchange and detected using a LC-MS system with electrospray...

  7. Involvement of a Natural Fusion of a Cytochrome P450 and a Hydrolase in Mycophenolic Acid Biosynthesis

    DEFF Research Database (Denmark)

    Hansen, Bjarne Gram; Mnich, Ewelina; Nielsen, Kristian Fog;

    2012-01-01

    Mycophenolic acid (MPA) is a fungal secondary metabolite and the active component in several immunosuppressive pharmaceuticals. The gene cluster coding for the MPA biosynthetic pathway has recently been discovered in Penicillium brevicompactum, demonstrating that the first step is catalyzed by Mp....... Overall, the chimeric enzyme MpaDE provides insight into the genetic organization of the MPA biosynthesis pathway.......DNA prepared from the extracted RNA. Heterologous coexpression of mpaC and the fusion gene mpaDE in the MPA-nonproducer Aspergillus nidulans resulted in the production of 5,7-dihydroxy-4-methylphthalide (DHMP), the second intermediate in MPA biosynthesis. Analysis of the strain coexpressing mpaC and the mpa...

  8. Effects of Mycophenolic Acid on High Glucose-induced Expression of TGF-β and CTGF in Mesangial Cells

    Institute of Scientific and Technical Information of China (English)

    L(U) Yongman; CHEN Junying; SHAO Jufang

    2006-01-01

    The effects of mycophenolic acid (MPA) on high glucose-induced expression of transforming growth factor-β (TGF-β) and connective tissue growth factor (CTGF) in mesangial cells (MC) were investigated. Rat MC were cultured in the presence of different concentrations of MPA (1.0 and 10.0 μmol/L) or MPA plus high glucose for 72 h. The expression of TGF-β and CTGF was detected by Western blot. The results showed that high glucose could induce the expression of TGF-β and CTGF in MC, but MPA could inhibit this effects. MPA did not influence the expression of TGF-β and CTGF in normal glucose. It was concluded that MPA might prevent the progression of diabetic nephropathy by inhibiting the expression of TGF-β and CTGF in MC.

  9. Mycophenolic acid, an immunomodulator, has potent and broad-spectrum in vitro antiviral activity against pandemic, seasonal and avian influenza viruses affecting humans.

    Science.gov (United States)

    To, Kelvin K W; Mok, Ka-Yi; Chan, Andy S F; Cheung, Nam N; Wang, Pui; Lui, Yin-Ming; Chan, Jasper F W; Chen, Honglin; Chan, Kwok-Hung; Kao, Richard Y T; Yuen, Kwok-Yung

    2016-08-01

    Immunomodulators have been shown to improve the outcome of severe pneumonia. We have previously shown that mycophenolic acid (MPA), an immunomodulator, has antiviral activity against influenza A/WSN/1933(H1N1) using a high-throughput chemical screening assay. This study further investigated the antiviral activity and mechanism of action of MPA against contemporary clinical isolates of influenza A and B viruses. The 50 % cellular cytotoxicity (CC50) of MPA in Madin Darby canine kidney cell line was over 50 µM. MPA prevented influenza virus-induced cell death in the cell-protection assay, with significantly lower IC50 for influenza B virus B/411 than that of influenza A(H1N1)pdm09 virus H1/415 (0.208 vs 1.510 µM, P=0.0001). For H1/415, MPA interfered with the early stage of viral replication before protein synthesis. For B/411, MPA may also act at a later stage since MPA was active against B/411 even when added 12 h post-infection. Virus-yield reduction assay showed that the replication of B/411 was completely inhibited by MPA at concentrations ≥0.78 µM, while there was a dose-dependent reduction of viral titer for H1/415. The antiviral effect of MPA was completely reverted by guanosine supplementation. Plaque reduction assay showed that MPA had antiviral activity against eight different clinical isolates of A(H1N1), A(H3N2), A(H7N9) and influenza B viruses (IC50 <1 µM). In summary, MPA has broad-spectrum antiviral activity against human and avian-origin influenza viruses, in addition to its immunomodulatory activity. Together with a high chemotherapeutic index, the use of MPA as an antiviral agent should be further investigated in vivo. PMID:27259985

  10. Human α/β hydrolase domain containing 10 (ABHD10) is responsible enzyme for deglucuronidation of mycophenolic acid acyl-glucuronide in liver.

    Science.gov (United States)

    Iwamura, Atsushi; Fukami, Tatsuki; Higuchi, Ryota; Nakajima, Miki; Yokoi, Tsuyoshi

    2012-03-16

    Mycophenolic acid (MPA), the active metabolite of the immunosuppressant mycophenolate mofetil (MMF), is primarily metabolized by glucuronidation to a phenolic glucuronide (MPAG) and an acyl glucuronide (AcMPAG). It is known that AcMPAG, which may be an immunotoxic metabolite, is deglucuronidated in human liver. However, it has been reported that recombinant β-glucuronidase does not catalyze this reaction. AcMPAG deglucuronidation activity was detected in both human liver cytosol (HLC) and microsomes (HLM). In this study, the enzyme responsible for AcMPAG deglucuronidation was identified by purification from HLC with column chromatographic purification steps. The purified enzyme was identified as α/β hydrolase domain containing 10 (ABHD10) by amino acid sequence analysis. Recombinant ABHD10 expressed in Sf9 cells efficiently deglucuronidated AcMPAG with a K(m) value of 100.7 ± 10.2 μM, which was similar to those in HLM, HLC, and human liver homogenates (HLH). Immunoblot analysis revealed ABHD10 protein expression in both HLC and HLM. The AcMPAG deglucuronidation by recombinant ABHD10, HLC, and HLH were potently inhibited by AgNO(3), CdCl(2), CuCl(2), PMSF, bis-p-nitrophenylphosphate, and DTNB. The CL(int) value of AcMPAG formation from MPA, which was catalyzed by human UGT2B7, in HLH was increased by 1.8-fold in the presence of PMSF. Thus, human ABHD10 would affect the formation of AcMPAG, the immunotoxic metabolite. PMID:22294686

  11. Mycophenolate mofetil: safety and efficacy in the prophylaxis of acute kidney transplantation rejection

    Directory of Open Access Journals (Sweden)

    Pranav Dalal

    2009-01-01

    Full Text Available Pranav Dalal1, Monica Grafals2, Darshika Chhabra2, Lorenzo Gallon21Department of Medicine, Mount Sinai Hospital, Chicago, USA; 2Northwestern University–Feinberg School of Medicine, Chicago, USAAbstract: Mycophenolate mofetil (MMF, a prodrug of mycophenolic acid (MPA, is an inhibitor of inosine monophosphate dehydrogenase (IMPDH. It preferentially inhibits denovo pathway of guanosine nucleotide synthesis in T and B-lymphocytes and prevents their proliferation, thereby suppresses both cell mediated and humoral immune responses. Clinical trials in kidney transplant recipients have shown the efficacy of MMF in reducing the incidence and severity of acute rejection episodes. It also improves long term graft function as well as graft and patient survival in kidney transplant recipients. MMF is useful as a component of toxicity sparing regimens to reduce or avoid exposure of steroids or calcineurin inhibitor (CNI. Enteric-coated mycophenolate sodium (EC-MPS can be used as an alternative immunosuppressive agent in kidney transplant recipients with efficacy and safety profile similar to MMF.Keywords: mycophenolate mofetil, kidney transplantation, acute rejection, toxicity sparing

  12. Bayesian estimation of mycophenolate mofetil in lung transplantation, using a population pharmacokinetic model developed in kidney and lung transplant recipients.

    OpenAIRE

    De Winter, Brenda,; Monchaud, Caroline; Prémaud, Aurélie; Pison, Christophe; Kessler, Romain; Reynaud-Gaubert, Martine; Dromer, Claire; Stern, Marc,; Guillemain, Romain; Knoop, Christiane; Estenne, Marc; Marquet, Pierre; Rousseau, Annick

    2012-01-01

    BACKGROUND AND OBJECTIVES: The immunosuppressive drug mycophenolate mofetil is used to prevent rejection after organ transplantation. In kidney transplant recipients, it has been demonstrated that adjustment of the mycophenolate mofetil dose on the basis of the area under the concentration-time curve (AUC) of mycophenolic acid (MPA), the active moiety of mycophenolate mofetil, improves the clinical outcome. Because of the high risks of rejections and infections in lung transplant recipients, ...

  13. Performance of the Roche Total Mycophenolic Acid® assay on the Cobas Integra 400®, Cobas 6000® and comparison to LC-MS/MS in liver transplant patients

    OpenAIRE

    Decavele, An-Sofie; FAVOREEL, NIELS; VANDER HEYDEN, FIEN; Verstraete, Alain

    2011-01-01

    Background: Mycophenolic acid (MPA) is an immunosuppressant for which therapeutic drug monitoring (TDM) is performed for optimal prophylaxis and avoidance of toxicity in transplant patients. Liquid chromatography-tandem mass spectrometry (LC-MS/MS) is ideally suited for TDM of MPA. There have been several method comparisons of the Roche Total MPA assay, but none have been performed with respect to liver transplant patients. Methods: We validated the Roche Total MPA assay on the Cobas Inte...

  14. 霉酚酸高产菌株短密青霉菌的选育%Selection for mycophenolic acid high-producing Penicillium brevicompactum

    Institute of Scientific and Technical Information of China (English)

    廖爱芳; 陈宏; 贾纬

    2011-01-01

    Objective To breed high producing strain of mycophenolic acid. Methods Penicillium brevicompactum UH35-58 was used as starting strain and treated by UV mutagenesis. The procedure, 20% water was fed after culturing 64 hours by flask-shaking fermentation, was adopted as preliminary screening to eliminate much of the low yield mutants. The titer of the culture was measured by HPLC method. Results and Conclusion A high-yield mutant N110-N76 with the titer increased 120% was obtained from the parent strain UH35-58. The subculture test indicated that the hereditary character of strain Nl 10-N76 was stable.%以短密青霉菌UH35-58为出发菌株,紫外线为诱变剂,采用摇瓶一级发酵补水工艺(64h补水20%)淘汰大量低产菌株,获得高产突变株N110-N76.用HPLC测定其发酵液的霉酚酸含量,发酵单位比出发菌株UH35-58提高120%.经过连续传代试验,该菌株的遗传性状稳定.

  15. Mycophenolic acid induces ATP-binding cassette transporter A1 (ABCA1) expression through the PPARγ–LXRα–ABCA1 pathway

    International Nuclear Information System (INIS)

    Highlights: ► Using an ABCA1p-LUC HepG2 cell line, we found that MPA upregulated ABCA1 expression. ► MPA induced ABCA1 and LXRα protein expression in HepG2 cells. ► PPARγ antagonist GW9662 markedly inhibited MPA-induced ABCA1 and LXRα protein expression. ► The effect of MPA upregulating ABCA1 was due mainly to activation of the PPARγ-LXRα-ABCA1 pathway. -- Abstract: ATP-binding cassette transporter A1 (ABCA1) promotes cholesterol and phospholipid efflux from cells to lipid-poor apolipoprotein A-I and plays an important role in atherosclerosis. In a previous study, we developed a high-throughput screening method using an ABCA1p-LUC HepG2 cell line to find upregulators of ABCA1. Using this method in the present study, we found that mycophenolic acid (MPA) upregulated ABCA1 expression (EC50 = 0.09 μM). MPA upregulation of ABCA1 expression was confirmed by real-time quantitative reverse transcription-PCR and Western blot analysis in HepG2 cells. Previous work has indicated that MPA is a potent agonist of peroxisome proliferator-activated receptor gamma (PPARγ; EC50 = 5.2–9.3 μM). Liver X receptor α (LXRα) is a target gene of PPARγ and may directly regulate ABCA1 expression. Western blot analysis showed that MPA induced LXRα protein expression in HepG2 cells. Addition of PPARγ antagonist GW9662 markedly inhibited MPA-induced ABCA1 and LXRα protein expression. These data suggest that MPA increased ABCA1 expression mainly through activation of PPARγ. Thus, the effects of MPA on upregulation of ABCA1 expression were due mainly to activation of the PPARγ–LXRα–ABCA1 signaling pathway. This is the first report that the antiatherosclerosis activity of MPA is due to this mechanism.

  16. Mycophenolic acid induces ATP-binding cassette transporter A1 (ABCA1) expression through the PPAR{gamma}-LXR{alpha}-ABCA1 pathway

    Energy Technology Data Exchange (ETDEWEB)

    Xu, Yanni; Lai, Fangfang; Xu, Yang; Wu, Yexiang; Liu, Qi; Li, Ni; Wei, Yuzhen; Feng, Tingting; Zheng, Zhihui; Jiang, Wei; Yu, Liyan; Hong, Bin [Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050 (China); Si, Shuyi, E-mail: sisyimb@hotmail.com [Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050 (China)

    2011-11-04

    Highlights: Black-Right-Pointing-Pointer Using an ABCA1p-LUC HepG2 cell line, we found that MPA upregulated ABCA1 expression. Black-Right-Pointing-Pointer MPA induced ABCA1 and LXR{alpha} protein expression in HepG2 cells. Black-Right-Pointing-Pointer PPAR{gamma} antagonist GW9662 markedly inhibited MPA-induced ABCA1 and LXR{alpha} protein expression. Black-Right-Pointing-Pointer The effect of MPA upregulating ABCA1 was due mainly to activation of the PPAR{gamma}-LXR{alpha}-ABCA1 pathway. -- Abstract: ATP-binding cassette transporter A1 (ABCA1) promotes cholesterol and phospholipid efflux from cells to lipid-poor apolipoprotein A-I and plays an important role in atherosclerosis. In a previous study, we developed a high-throughput screening method using an ABCA1p-LUC HepG2 cell line to find upregulators of ABCA1. Using this method in the present study, we found that mycophenolic acid (MPA) upregulated ABCA1 expression (EC50 = 0.09 {mu}M). MPA upregulation of ABCA1 expression was confirmed by real-time quantitative reverse transcription-PCR and Western blot analysis in HepG2 cells. Previous work has indicated that MPA is a potent agonist of peroxisome proliferator-activated receptor gamma (PPAR{gamma}; EC50 = 5.2-9.3 {mu}M). Liver X receptor {alpha} (LXR{alpha}) is a target gene of PPAR{gamma} and may directly regulate ABCA1 expression. Western blot analysis showed that MPA induced LXR{alpha} protein expression in HepG2 cells. Addition of PPAR{gamma} antagonist GW9662 markedly inhibited MPA-induced ABCA1 and LXR{alpha} protein expression. These data suggest that MPA increased ABCA1 expression mainly through activation of PPAR{gamma}. Thus, the effects of MPA on upregulation of ABCA1 expression were due mainly to activation of the PPAR{gamma}-LXR{alpha}-ABCA1 signaling pathway. This is the first report that the antiatherosclerosis activity of MPA is due to this mechanism.

  17. SYNTHESIS OF MYCOPHENOLIC ACID (MPA)

    DEFF Research Database (Denmark)

    2008-01-01

    The present invention relates to novel tools for improving MPA production. In particular, the present invention relates tofungal enzymes that are specific for MPA synthesis.......The present invention relates to novel tools for improving MPA production. In particular, the present invention relates tofungal enzymes that are specific for MPA synthesis....

  18. Mycophenolate mofetil as adjuvant in pemphigus vulgaris

    Directory of Open Access Journals (Sweden)

    Sarma Nilendu

    2007-01-01

    Full Text Available Pemphigus vulgaris (PV is a life threatening autoimmune blistering disease of skin and mucous membranes. Advent of systemic steroids has greatly reduced the mortality rate. However, steroids and adjuvant immunosuppressive therapy are nowadays frequent contributory agents of morbidity and mortality of PV. Mycophenolate mofetil (MMF has been reported to be an effective adjuvant to systemic steroids. It helps in increasing the immunosuppressive effect and minimizing the toxicities by steroid sparing effect. However, its efficacy in refractory cases of PV is not well documented. The lowest possible dose with satisfactory therapeutic efficacy and least side effects is known. We used MMF 1 g/day and systemic steroids in 3 Indian patients with pemphigus vulgaris who were resistant to systemic steroid monotherapy or combination treatment with azathioprine. In our experience, MMF offers an effective adjuvant with minimal side-effects in the treatment of resistant PV.

  19. Mycophenolate mofetil: safety and efficacy in the prophylaxis of acute kidney transplantation rejection

    OpenAIRE

    Pranav Dalal; Monica Grafals; Darshika Chhabra; Lorenzo Gallon

    2009-01-01

    Pranav Dalal1, Monica Grafals2, Darshika Chhabra2, Lorenzo Gallon21Department of Medicine, Mount Sinai Hospital, Chicago, USA; 2Northwestern University–Feinberg School of Medicine, Chicago, USAAbstract: Mycophenolate mofetil (MMF), a prodrug of mycophenolic acid (MPA), is an inhibitor of inosine monophosphate dehydrogenase (IMPDH). It preferentially inhibits denovo pathway of guanosine nucleotide synthesis in T and B-lymphocytes and prevents their proliferation, thereby suppresses b...

  20. Mycophenolate mofetil attenuates pulmonary arterial hypertension in rats

    International Nuclear Information System (INIS)

    Pulmonary arterial hypertension (PAH) is characterized by abnormal proliferation of smooth muscle cells (SMCs), leading to occlusion of pulmonary arterioles, right ventricular (RV) hypertrophy, and death. We investigated whether mycophenolate mofetil (MMF), a potent immunosuppresssant, prevents the development of monocrotaline (MCT)-induced PAH in rats. MMF effectively decreased RV systolic pressure and RV hypertrophy, and reduced the medial thickness of pulmonary arteries. MMF significantly inhibited the number of proliferating cell nuclear antigen (PCNA)-positive cells, infiltration of macrophages, and expression of P-selectin and interleukin-6 on the endothelium of pulmonary arteries. The infiltration of T cells and mast cells was not affected by MMF. In vitro experiments revealed that mycophenolic acid (MPA), an active metabolite of MMF, dose-dependently inhibited proliferation of human pulmonary arterial SMCs. MMF attenuated the development of PAH through its anti-inflammatory and anti-proliferative properties. These findings provide new insight into the potential role of immunosuppressants in the treatment of PAH

  1. The Role of the Immunosuppressant Mycophenolate Mofetil in Pediatric Renal Transplant Recipients

    Directory of Open Access Journals (Sweden)

    M. Oellerich

    2004-04-01

    Full Text Available The immunosuppressive agent mycophenolate mofetil (MMF is being used since 1996 also in pediatric renal transplant recipients. There is no doubt that MMF is of clinical benefit in the initial posttransplant period in pediatric renal transplant recipients. Two multicenter trials have provided evidence that MMF at the daily dose of 1200 mg/m² body surface area given in two divided doses in conjunction with cyclosporin A (CsA and prednisolone is superior to azathioprine in the pediatric renal transplant population. The tolerability of MMF in children is in general acceptable; the most frequent side effects necessitating dosage reduction are diarrhea and/or nausea and leukopenia. Some arguments for giving MMF as a long-term maintenance immunosuppressive agent are based on what it does not do: it does not cause lipid or carbohydrate metabolism abnormalities or organ toxicity (e.g., hepatotoxicity, nephrotoxicity, or neurotoxicity, it is not mutagenic, and it does not inhibit longitudinal growth. MMF is sufficiently powerful to allow a decrease of potentially nephrotoxic CsA in the stable phase posttransplant in children with chronic transplant nephropathy without the burden of acute rejection, and there is growing evidence for a steroid sparing potential of MMF in this patient population. The therapeutic potential of MMF may be optimized in the future by therapeutic drug monitoring. The estimation of mycophenolic acid (MPA exposure in children is probably best achieved by use of an abbreviated area under the concentration curve. A large multicenter prospective randomized FDCC-study involving both adult and pediatric renal transplant recipients is currently investigating whether a concentration-controlled (CC dosing of MMF is superior to a fixed dose (FD regimen regarding efficacy and tolerability.

  2. 毛细管区带电泳测定人血浆中麦考酚酸浓度%A simple capillary zone electrophoresis method for the determination of mycophenolic acid in human plasma

    Institute of Scientific and Technical Information of China (English)

    熊祯; 段京莉; 翟所迪; 赵磊; 徐彭

    2009-01-01

    建立了人血浆中麦考酚酸浓度的毛细管区带电泳测定法.200μL的血浆样品经400μL的乙腈沉淀蛋白后,紧接一段水柱进样,进样量为:0.5 psi×10s.分离采用内径75μm,有效长度50 cm的未涂层熔硅弹性石英毛细管柱.通过均匀设计实验,选定pH为8.60的硼酸缓冲液(硼酸初始浓度为200 mmol/L)为背景缓冲液.结果显示,测定方法的标准曲线在0.625~30.0 μm/mL.的范围内,r平均值大于0.9997;检测下限为0.200μg/mL;日内、日间精密度均小于4.45%.应用本方法和高效液相色谱.串联质谱法,对14份接受麦考酚酸酯治疗的肾移植术后患者的血样进行分析.表明本方法准确、精密、经济,对于麦考酚酸的临床定量极具价值.%Mycophenolic acid (MPA), an immunosuppressive drug, was determined in human plasma by a simple capillary zone electrophoresis (CZE) method. A bare fused-silica capillary with an internal diameter (i.d.) of 75 μm and an effective length of 50 cm was used for the separation. A 200 μL plasma sample was deproteinized with 400 uL acetonitrile, and the supernatant was directly injected into the capillary after a water plug at a pressure of 0.5 psi for 10 s. Boric acid (H3BO3, 200 mmol/L) solution adjusted to a pH of 8.60 with 1 mol/L sodium hydroxide (NaOH) solution was selected as the background electrolyte (BGE) through a uniform design. Calibration curve established on each day was linear over the MPA concentration range of 0.625-30.0 ug/mL in human plasma with the correlation coefficient (r) larger than 0.9997. The limit of detection (LOD) was 0.200 μg/mL. Intra-and inter-day precisions at three concentrations within the calibration range were less than 4.45%. Plasma samples collected from 14 renal transplant recipients treated with the prodrug mycophenolate mofetil (MMF) were analyzed successfully by both the developed CZE technique and a validated high-performance liquid chromatography-tandem mass spectrometry (HPLC

  3. 血霉酚酸水平监测在肾移植临床的应用现状及进展%Therapeutic drug monitoring of mycophenolic acid in renal transplantation

    Institute of Scientific and Technical Information of China (English)

    张桓熙; 刘岩峰; 王长希

    2011-01-01

    This review aims to summarize the latest researches on therapeutic drug monitoring of mycophenolic acid, forming the basis for the proper prescription of Mycophenolic Acid ( MPA) and the optimization of anti-rejection medication for Chinese. The technology of measuring the total and free MPA concentration in the plasma includes high-performance liquid chromatography with ultraviolet detector,fluorescence detector and tandem mass spectrometer respectively,and enzyme-multiplied immunoassay technique. Either MMF or EC-MPS can be absorbed by the gastrointestinal tract and metabolized into MPA,whose main metabolite is MPAG. MPA displays large between- and within-subject pharmacokinetic variability. The pharmacokinetics of MPA is mainly interfered with by race, plasmic albumin concentration,the renal function,food,and interactions with other immunosuppressant drug. Low MPA AUC or trough concentration may increase the risk of acute rejection,while the high ones may cause more adverse effects. In TDM,MPA AUC should be maintained between 30 and 60 mg · h · L-1. The monitoring of free MPA may provide greater predictive value in terms of adverse effects. TDM actually helps the clinicians to adjust the MPA dose more appropriately,although it is still controversial whether TDM benefits the patients or not%本综述通过总结近几年霉酚酸(MPA)水平监测的研究进展,为进一步合理使用MPA并探究如何优化国人抗排斥方案提供线索.MPA检测方法分为高效液相色谱法(HPLC)和酶免疫分析法(EIA),其中HPLC联用紫外检测器、荧光检测器或串联质谱,和EMIT可测定MPA总浓度和游离浓度.MPA可通过MMF或EC-MPS经胃肠道吸收代谢转化而得,主要代谢物为MPAG.MPA的代谢存在明显的个体内和个体间差异,影响因素主要包括种族,血浆白蛋白浓度,移植肾功能,进食和药物配伍.低MPA AUC或谷浓度值会增加急性排斥的风险,高MPA AUC或谷浓度值会增加发生不良反应的风

  4. Salicylic acid as a peeling agent: a comprehensive review

    OpenAIRE

    Arif T

    2015-01-01

    Tasleem Arif Postgraduate Department of Dermatology, STD and Leprosy, Government Medical College, Srinagar, Jammu and Kashmir, India Abstract: Salicylic acid has been used to treat various skin disorders for more than 2,000 years. The ability of salicylic acid to exfoliate the stratum corneum makes it a good agent for peeling. In particular, the comedolytic property of salicylic acid makes it a useful peeling agent for patients with acne. Once considered as a keratolytic agent, the role of s...

  5. Salicylic acid as a peeling agent: a comprehensive review

    Directory of Open Access Journals (Sweden)

    Arif T

    2015-08-01

    Full Text Available Tasleem Arif Postgraduate Department of Dermatology, STD and Leprosy, Government Medical College, Srinagar, Jammu and Kashmir, India Abstract: Salicylic acid has been used to treat various skin disorders for more than 2,000 years. The ability of salicylic acid to exfoliate the stratum corneum makes it a good agent for peeling. In particular, the comedolytic property of salicylic acid makes it a useful peeling agent for patients with acne. Once considered as a keratolytic agent, the role of salicylic acid as a desmolytic agent, because of its ability to disrupt cellular junctions rather than breaking or lysing intercellular keratin filaments, is now recognized and is discussed here. Salicylic acid as a peeling agent has a number of indications, including acne vulgaris, melasma, photodamage, freckles, and lentigines. The efficacy and safety of salicylic acid peeling in Fitzpatrick skin types I–III as well as in skin types V and VI have been well documented in the literature. This paper reviews the available data and literature on salicylic acid as a peeling agent and its possible indications. Its properties, efficacy and safety, the peeling procedure, and possible side effects are discussed in detail. An account of salicylism is also included. Keywords: acne vulgaris, desmolytic agent, melasma, photodamage, salicylic acid 

  6. Randomised trial of mycophenolate mofetil versus azathioprine for treatment of chronic active Crohn's disease

    OpenAIRE

    Neurath, M; Wanitschke, R; Peters, M.; Krummenauer, F; zum, B; Schlaak, J.

    1999-01-01

    BACKGROUND—Crohn's disease is a chronic inflammatory disease of the alimentary tract. Azathioprine is an effective agent in the management of chronic active Crohn's disease leading to long term remission of disease activity. Such treatment leads to limited efficacy or side effects in a small subset of patients. 
AIMS—To compare efficacy and side effects of treatment with azathioprine plus corticosteroids versus mycophenolate mofetil (MMF) plus corticosteroids in patients wit...

  7. Functional Distinctions between IMP Dehydrogenase Genes in Providing Mycophenolate Resistance and Guanine Prototrophy to Yeast*

    OpenAIRE

    Hyle, Judith W.; Shaw, Randal J.; Reines, Daniel

    2003-01-01

    IMP dehydrogenase (IMPDH) catalyzes the rate-limiting step in the de novo synthesis of GTP. Yeast with mutations in the transcription elongation machinery are sensitive to inhibitors of this enzyme such as 6-azauracil and mycophenolic acid, at least partly because of their inability to transcriptionally induce IMPDH. To understand the molecular basis of this drug-sensitive phenotype, we have dissected the expression and function of a four-gene family in yeast called IMD1 through IMD4. We show...

  8. Guanidinoacetic acid as a performance-enhancing agent.

    Science.gov (United States)

    Ostojic, Sergej M

    2016-08-01

    Guanidinoacetic acid (GAA; also known as glycocyamine or guanidinoacetate) is the natural precursor of creatine, and under investigation as a novel dietary agent. It was first identified as a natural compound in humans ~80 years ago. In the 1950s, GAA's use as a therapeutic agent was explored, showing that supplemental GAA improved patient-reported outcomes and work capacity in clinical populations. Recently, a few studies have examined the safety and efficacy of GAA and suggest potential ergogenic benefits for physically active men and women. The purpose of this review is to examine possible applications of GAA supplementation for exercise performance enhancement, safety, and legislation issues. PMID:26445773

  9. Mycophenolate mofetil alters the antioxidant status in duodenum of rats: Implication for silymarin usage in mycophenolate mofetil induced gastrointestinal disorders

    Directory of Open Access Journals (Sweden)

    Sanaz Sheikhzadeh

    2013-06-01

    Full Text Available Mycophenolate mofetil (MMF as an immunosuppressive agent is used to prevent graftrejection. One of the adverse effects of long time administration of MMF is the gastrointestinaldisorder. This study aimed to investigate the gastroprotective effect of silymarin (SMN onMMF-induced gastrointestinal (GI disorders. Twenty-four adult female Wistar rats wereassigned into three groups including the control and test groups. The control animals receivedsaline(5 mL kg-1andthe test animals were treated with MMF (40 mg kg-1, orally and saline,MMF and silymarin (SMN, 50 mg kg-1, orally for 14 consecutive days, respectively. To evaluatethe GI disorders due to the MMF-induced oxidative stress and subsequently the protective effectof SMN, malondialdehyde (MDA,total thiol molecules(TTM levels and total anti-oxidantcapacity (TAC were determined. Additionally, histopathological examinations in the duodenalregion of small intestine were performed. The MMF-increased level of MDA was reduced bySMN administration, while the MMF-reduced level of TTM increased significantly (p< 0.05 bySMN administration. Histopathological examinations showed the goblet cell reduction andcongestion in the MMF-received animals; while SMN was able to improve the MMF-inducedgoblet cell reduction and congestion. Our data suggest that the MMF-induced GI disorders arecharacterized by changes in antioxidant status, which presented by the elevation of MDA leveland reduction of TTM concentration. Moreover, the improved biochemical alterations andhistopathologic damages by SMN indicating its gastroprotective and antioxidant effects

  10. Bile acids as endogenous etiologic agents in gastrointestinal cancer

    Institute of Scientific and Technical Information of China (English)

    Harris Bernstein; Carol Bernstein; Claire M Payne; Katerina Dvorak

    2009-01-01

    Bile acids are implicated as etiologic agents in cancer of the gastrointestinal (GI) tract, including cancer of the esophagus, stomach, small intestine, liver, biliary tract, pancreas and colon/rectum. Deleterious effects of bile acid exposure, likely related to carcinogenesis,include: induction of reactive oxygen and reactive nitrogen species; induction of DNA damage; stimulation of mutation; induction of apoptosis in the short term,and selection for apoptosis resistance in the long term.These deleterious effects have, so far, been reported most consistently in relation to esophageal and colorectal cancer, but also to some extent in relation to cancer of other organs. In addition, evidence is reviewed for an association of increased bile acid exposure with cancer risk in human populations, in specific human genetic conditions, and in animal experiments. A model for the role of bile acids in GI carcinogenesis is presented from a Darwinian perspective that offers an explanation for how the observed effects of bile acids on cells contribute to cancer development.

  11. Gradual surface degradation of restorative materials by acidic agents.

    Science.gov (United States)

    Hengtrakool, Chanothai; Kukiattrakoon, Boonlert; Kedjarune-Leggat, Ureporn

    2011-01-01

    The aim of this study was to investigate the effect of acidic agents on surface roughness and characteristics of four restorative materials. Fifty-two discs were created from each restorative material: metal-reinforced glass ionomer cement (Ketac-S), resin-modified glass ionomer cement (Fuji II LC), resin composite (Filtek Z250), and amalgam (Valiant-PhD); each disc was 12 mm in diameter and 2.5 mm thick. The specimens were divided into four subgroups (n=13) and immersed for 168 hours in four storage media: deionized water (control); citrate buffer solution; green mango juice; and pineapple juice. Surface roughness measurements were performed with a profilometer, both before and after storage media immersion. Surface characteristics were examined using scanning electron microscopy (SEM). Statistical significance among each group was analyzed using two-way repeated ANOVA and Tukey's tests. Ketac-S demonstrated the highest roughness changes after immersion in acidic agents (pValiant-PhD and Filtek Z250 illustrated some minor changes over 168 hours. The mango juice produced the greatest degradation effect of all materials tested (p<0.05). SEM photographs demonstrated gradual surface changes of all materials tested after immersions. Of the materials evaluated, amalgam and resin composite may be the most suitable for restorations for patients with tooth surface loss. PMID:21903509

  12. Successful treatment of severe refractory lupus hepatitis with mycophenolate mofetil.

    Science.gov (United States)

    Tagawa, Y; Saito, T; Takada, K; Kawahata, K; Kohsaka, H

    2016-04-01

    Systemic lupus erythematosus-related hepatitis, known as lupus hepatitis, is a rare manifestation of systemic lupus erythematosus, and is usually subclinical with mild abnormalities of serum liver enzymes. While cases with clinically significant and refractory lupus hepatitis are uncommon, treatment options for lupus hepatitis are to be established. Here, we report the case of a 45-year-old man with progressive lupus hepatitis accompanied by autoimmune haemolytic anaemia. Lupus hepatitis of this patient was refractory to tacrolimus, azathioprine and cyclophosphamide, but was successfully treated by mycophenolate mofetil. Mycophenolate mofetil might be an effective therapeutic option for refractory lupus hepatitis. PMID:26762472

  13. Mechanisms of oxide dissolution by acid chelating agents

    International Nuclear Information System (INIS)

    In this paper, the different possible rate controlling processes in the dissolution of metallic oxides are examined. In particular, the following situations are assessed: mass-transfer control; coupling of mass-transfer and reactions at the interface; interface equilibration with the solution; various interface disruption and reconstruction phenomena. For each of the above mentioned cases, the influence of variables such as reagent concentration, temperature, pH, fluid hydrodynamics and general and specific catalysts is discussed. Depending upon the particular situation it is found that a more rational basis for the development of reagent is given by these considerations. The influence of chelating agents on both the thermodynamics and kinetics of the process is discussed, and the results of experimental studies in batch on magnetite and various ferrites are presented and discussed. For this purpose, several reagents were studied, including some very effective ones like thioglycolic acid, and others commonly used in actual decontamination, like ethylenediaminetetraacetic acid and oxalic acid. The relation to other (reductive) chemical decontamination procedures is discussed. The relevance of these studies to decontamination of metallic surfaces is discussed

  14. Treatment of severe henoch-schonlein purpura nephritis with mycophenolate mofetil

    Directory of Open Access Journals (Sweden)

    Ahmad Ali Nikibakhsh

    2014-01-01

    Full Text Available Henoch-Schonlein purpura (HSP is the most common childhood vasculitis. Renal involvement in HSP is one of the major causes of chronic renal failure in children. It is important to start effective and relatively safe medication to prevent end-stage renal disease (ESRD. Mycophenolate mofetil (MMF appears to be a promising therapeutic agent in many autoimmune diseases such as lupus nephritis and vasculitis. Herein, we describe the treatment with MMF of three patients with HSP nephritis. In two cases with rapidly progressive glomerulonephritis without response to steroid, after treatment with MMF, significant improvement in kidney function and proteinuria were observed. In another patient with HSP nephritic-nephrotic syn-drome who showed resistance to steroid, MMF offered a favorable effect. MMF seems to be a promising therapeutic agent in the treatment of the severe HSP nephritis.

  15. Mycophenolate mofetil in erosive genital lichen planus: a case and review of the literature.

    Science.gov (United States)

    Deen, Kristyn; McMeniman, Erin

    2015-03-01

    Erosive genital lichen planus is a disabling, inflammatory mucocutaneous condition that can cause significant patient morbidity and loss of function. Treatment initially involves topical corticosteroids but some patients can have severe treatment-resistant courses requiring systemic immunosuppression. With potentially unfavorable adverse effect profiles and subsequent intolerance of these agents by patients, erosive lichen planus can ultimately be a challenging condition to treat effectively. We present a case of a 66-year-old woman with treatment-resistant erosive genital lichen planus who was successfully managed with mycophenolate mofetil. Although there is only weak evidence for this agent in this condition, its role in dermatology is growing due to its efficacy and advantageous adverse effect profile and should therefore be considered in patients with treatment-resistant erosive genital lichen planus. PMID:25583369

  16. Mycophenolate mofetil in the treatment of non-renal manifestations of systemic lupus erythematosus: recent insights

    Directory of Open Access Journals (Sweden)

    Ali SAHIN

    2010-05-01

    Full Text Available Mycophenolate mofetil (MMF is an immunosuppressive agent that has been shown to beeffective in transplant patients. It is also efficacious in the management of lupus nephritis, anduseful in the treatment of autoimmune conditions as its mechanisms of action target the T- andB – lymphocytes, leading to suppression of the cell-mediated 3immune responses and antibodyformation. It has been used successfully in immune-mediated conditions like myasthenia gravis,autoimmune hepatitis and immune cytopenias. However, its optimal use in non-renalmanifestations (hematological, neuropsychiatric, myocardial, pulmonary, cutaneous etc. inlupus patients is unclear. There are yet to be randomised controlled trials to guide the optimaldoses and durations of MMF in such situations. MMF is well tolerated and safe to use, thoughthere are reports of serious adverse effects like urticaria, myopathy, Epstein-Barr virus-associatedB-cell lymphoma, cytomegalovirus infections and disseminated varicella zoster. Another areaof concern for patients is the increased cost of using long-term MMF.Key words: systemic lupus erythematosus, mycophenolate mofetil, treatment.

  17. Enhancement of Mycophenolate Mofetil Permeation for Topical Use by Eucalyptol and N-Methyl-2-pyrrolidone

    Science.gov (United States)

    Songkram, Chalermkiat

    2016-01-01

    Mycophenolate mofetil (MMF) is a prodrug of mycophenolic acid (MPA) which can be metabolized by esterase. MMF has been approved by the United States Food and Drug Administration (USFDA) for treatment of psoriasis patient with skin symptoms. However, it remains unclear whether MMF is efficiently effective to treat skin symptoms developed from psoriasis. The insufficient amount of MMF penetrating through the skin results in the treatment failure due to the difficulty in MMF penetration through the stratum corneum. Skin permeation enhancers such as eucalyptol (EUL) and N-methyl-2-pyrrolidone (NMP) potentially aid in increasing skin penetration. This study aimed to investigate the effects of a concentration ratio (% w/v) between two enhancers (EUL and NMP). The results showed that EUL enhanced MMF permeation with an enhancement ratio (ER) of 3.44 while NMP was not able to promote the penetration of MMF. Interestingly, the synergistic effect of the two enhancers was observed with a suitable ratio given that the ER was 8.21. EUL and NMP are promising enhancers for the development of MMF based skin product. PMID:27069715

  18. Mycophenolate-Associated Alopecia in an Adolescent Girl Mycophenolate and Alopecia

    Directory of Open Access Journals (Sweden)

    Belde KASAP

    2014-01-01

    Full Text Available PURPOSE: To report a patient treated with enteric-coated mycophenolate sodium (EC-MPS, in whom infrequent side effects developed. CASE REPORT: A 14-year-old girl presented with hair loss after starting EC-MPS. She had her fi rst nephrotic syndrome attack when she was 7 years old. During the next six years, she had six attacks and two biopsies without fi ndings of segmental sclerosis. She received steroids and 55 months of CsA. She was evaluated as steroid and CsA dependent when she had a relapse a month after cessation of treatment. The last biopsy showed CsA toxicity. EC-MPS was institituted (1080 mg/d. Alopecia developed at the second month. The dose was decreased by two third and hair loss stopped within a month. Her menstrual cycles also ceased after EC-MPS treatment and resumed two months after dose reduction. She remained in remission during the following 8 months and had a new relapse thereafter, which responded to a short term of high dose steroid treatment. She is still on the 20th month of EC-MPS and had no relapse. CONCLUSION: This is the fi rst adolescent with alopecia and menstrual irregularity during EC-MPS treatment, which may be effective even at a two third of the suggested dose.

  19. Pulmonary alveolar proteinosis due to mycophenolate and cyclosporine combination therapy in a renal transplant recipient

    Directory of Open Access Journals (Sweden)

    Ashfaq Hasan

    2014-01-01

    Full Text Available Pulmonary alveolar proteinosis (PAP is an orphan disease characterized by the accumulation of excess of surfactant within alveoli and bronchioles. The primary form of PAP (P-PAP; also referred to as idiopathic or autoimmune is the most common form. It is mediated through a circulating neutralizing antibody against granulocyte-macrophage colony-stimulating factor. Secondary PAP (S-PAP can be induced by a host of inciting agents and is far more liable to progress to terminal respiratory failure. We describe a rare case of S-PAP occurring in a renal transplant recipient due to mycophenolate and cyclosporine combination-therapy, which resolved spontaneously following withdrawal of these drugs.

  20. Mycophenolate mofetil for drug-induced vanishing bile duct syndrome

    Institute of Scientific and Technical Information of China (English)

    2007-01-01

    Amoxicillin/clavulanate is associated with liver injury,mostly of a cholestatic pattern. While outcomes are usually benign, progression to cirrhosis and death has been reported. The role of immunosuppressive therapy for patients with a protracted course is unclear. We report the case of an elderly patient who developed prolonged cholestasis secondary to amoxicillin/clavulanate. Vanishing bile duct syndrome was confirmed by sequential liver biopsies. The patient responded to prednisone treatment,but could not be weaned off corticosteroids, even when azathioprine was added. Complete withdrawal of both prednisone and azathioprine was possible by using mycophenolate mofetil, an inosine monophosphate dehydrogenase inhibitor. Sustained remission has been maintained for more than 3 years with low-dose mycophenolate mofetil.

  1. The impact of everolimus versus mycophenolate on blood and lymphocyte cyclosporine exposure in heart-transplant recipients

    DEFF Research Database (Denmark)

    Gustafsson, Finn; Barth, David; Delgado, Diego H;

    2009-01-01

    . METHODS: Twelve-hour pharmacokinetic studies of whole-blood and intralymphocytic CsA concentrations were conducted in long-term heart-transplant recipients treated with mycophenolate mofetil (MMF) + CsA (n = 8) and everolimus + CsA (n = 9). RESULTS: There was a highly significant correlation between blood......BACKGROUND: Trough- or 2-h post-dose (C2) blood cyclosporine (CsA) concentrations are used for prediction of efficacy and toxicity of CsA in transplant recipients concomitantly treated with antiproliferative agents, but information on utility of blood CsA levels in patients treated with...

  2. Gentisic acid: a new stabilizer for low tin skeletal imaging agents: concise communication

    International Nuclear Information System (INIS)

    In vitro stabilization of low-tin bone-imaging agents has previously been achieved with ascorbic acid. In this study gentisic acid is shown to be an equally effective antioxidant for the (1-hydroxyethylidene) diphosphonate (HEDP) and hydroxymethylenediphosphonate (HMDP) skeletal agents. In vitro studies show less than 2% free sodium [/sup 99m/Tc] pertechnetate at 24 h with the gentisic acid stabilizer. Studies in guinea pigs at 3 and 24 h - whether with C-14- or H-3-labeled gentisic acid as stabilizer - show no alteration in the biodistribution of either skeletal imaging agent by the addition of the gentisic acid. Gentisic acid is a safe and effective stabilizer, and clinical studies have shown bioequivalency with ascorbic acid

  3. Spherical Nucleic Acids as Intracellular Agents for Nucleic Acid Based Therapeutics

    Science.gov (United States)

    Hao, Liangliang

    Recent functional discoveries on the noncoding sequences of human genome and transcriptome could lead to revolutionary treatment modalities because the noncoding RNAs (ncRNAs) can be applied as therapeutic agents to manipulate disease-causing genes. To date few nucleic acid-based therapeutics have been translated into the clinic due to challenges in the delivery of the oligonucleotide agents in an effective, cell specific, and non-toxic fashion. Unmodified oligonucleotide agents are destroyed rapidly in biological fluids by enzymatic degradation and have difficulty crossing the plasma membrane without the aid of transfection reagents, which often cause inflammatory, cytotoxic, or immunogenic side effects. Spherical nucleic acids (SNAs), nanoparticles consisting of densely organized and highly oriented oligonucleotides, pose one possible solution to circumventing these problems in both the antisense and RNA interference (RNAi) pathways. The unique three dimensional architecture of SNAs protects the bioactive oligonucleotides from unspecific degradation during delivery and supports their targeting of class A scavenger receptors and endocytosis via a lipid-raft-dependent, caveolae-mediated pathway. Owing to their unique structure, SNAs are able to cross cell membranes and regulate target genes expression as a single entity, without triggering the cellular innate immune response. Herein, my thesis has focused on understanding the interactions between SNAs and cellular components and developing SNA-based nanostructures to improve therapeutic capabilities. Specifically, I developed a novel SNA-based, nanoscale agent for delivery of therapeutic oligonucleotides to manipulate microRNAs (miRNAs), the endogenous post-transcriptional gene regulators. I investigated the role of SNAs involving miRNAs in anti-cancer or anti-inflammation responses in cells and in in vivo murine disease models via systemic injection. Furthermore, I explored using different strategies to construct

  4. Anti-AIDS Agents 69.1 Moronic Acid and Other Triterpene Derivatives as Novel Potent Anti-HIV Agents

    OpenAIRE

    Yu, Donglei; Sakurai, Yojiro; Chen, Chin-Ho; Chang, Fang-Rong; Huang, Li; Kashiwada, Yoshiki; Lee, Kuo-Hsiung

    2006-01-01

    In a continuing structure-activity relationship study of potent anti-HIV agents, seven new triterpene derivatives were designed, synthesized, and evaluated for in vitro antiviral activity. Among them, moronic acid derivatives 19, 20 and 21 showed significant activity in HIV-1 infected H9 lymphocytes. Compounds 19 and 20 were also evaluated against HIV-1 NL4−3 and drug resistant strains in the MT-4 cell line. Compounds 19 and 20 showed better antiviral profiles than the betulinic acid analog 8...

  5. Mycophenolic acid:a novel immunosuppressive drug%霉吩酸:一种新型免疫抑制剂

    Institute of Scientific and Technical Information of China (English)

    李红良; 任先达; 叶开和

    2001-01-01

    Mycophenolate acid is a novel immunosuppressive drug. Its target of action is the isomerⅡof inosine 5'-monophosphate dehydrogenase(IMPDH). It inhibits de nove purine synthesis and also decreases expression of adhesive molecule. It inhibits selectively the proliferation of lymphocyte, so that it has strong immunosuppressive effects on various rejections to allograft or xenograft, and on autoimmune diseases, and has the features of higher potency and lower toxicity.

  6. Neonatal anemia and hydrops fetalis after maternal mycophenolate mofetil use.

    Science.gov (United States)

    Tjeertes, I F A; Bastiaans, D E T; van Ganzewinkel, C J L M; Zegers, S H J

    2007-01-01

    After admitting a patient to our Neonatal Intensive Care with a severe anemia and an ear malformation, we ruled out any other cause than maternal medication use. Knowing she used mycophenolate mofetil during pregnancy, we looked for related articles. Two articles were found describing ear malformations, but no article was ever written about anemia caused by this medication. Consulting the international registers of drug effects through the National Institute for Public Health and the Environment, we found out that the anemia was never seen or reported before. PMID:17180133

  7. Oral retinoic acid metabolism blocking agent Rambazole for plaque psoriasis: an immunohistochemical study.

    NARCIS (Netherlands)

    Bovenschen, H.J.; Kooijmans-Otero, M.E.; Langewouters, A.M.G.; Vlijmen-Willems, I.M.J.J. van; Rens, D.W.A. van; Seyger, M.M.B.; Kerkhof, P.C.M. van de

    2007-01-01

    BACKGROUND: The novel systemic all-trans retinoic acid metabolism blocking agent (RAMBA) R115866 (Rambazole(TM); Barrier Therapeutics, Geel, Belgium; further referred to as rambazole) increases intracellular levels of endogenous all-trans retinoic acid (RA). Well-known effects of RA are normalizatio

  8. Comparative Assessment of Automated Nucleic Acid Sample Extraction Equipment for Biothreat Agents

    OpenAIRE

    Kalina, Warren Vincent; Douglas, Christina Elizabeth; Coyne, Susan Rajnik; Minogue, Timothy Devin

    2014-01-01

    Magnetic beads offer superior impurity removal and nucleic acid selection over older extraction methods. The performances of nucleic acid extraction of biothreat agents in blood or buffer by easyMAG, MagNA Pure, EZ1 Advanced XL, and Nordiag Arrow were evaluated. All instruments showed excellent performance in blood; however, the easyMAG had the best precision and versatility.

  9. Oleic acid-embedded nanoliposome as a selective tumoricidal agent.

    Science.gov (United States)

    Jung, Sujin; Lee, Sangah; Lee, Hyejin; Yoon, Jaejin; Lee, E K

    2016-10-01

    HAMLET (Human Alpha-lactalbumin Made LEthal to Tumor cell), a molecular complex of human α-lactalbumin and oleic acid, is known to have selective cytotoxic activity against certain types of tumors. This cytotoxicity is known to stem from water-insoluble oleic acid. In this study, we manufactured an alternative complex using liposome as an oleic acid delivery vesicle. We named this nanolipoplex LIMLET (LIposome Made LEthal to Tumor cell). The LIMLET vesicle contained approximately 90,200 oleic acid molecules inserted into its lipophilic phospholipid bilayer and had a nominal mean diameter of 127nm. Using a WST-1 assay, its cytotoxicity against two cancer cell lines, MDA-MB-231 (human breast cancer) and A549 (human lung cancer), were tested. The results were compared with that of a normal cell line, Vero (from monkey kidney). We found that (1) LIMLET showed distinctive cytotoxicity against A549 and MDA-MB-231 cells, whereas bare liposomes (containing no oleic acid) had no toxicity, even at high concentrations, and (2) LIMLET demonstrated selective, concentration-dependent toxicity against the cancer cells: the LD50 values of MDA-MB-231 and A549 cells were 1.3 and 2.2nM LIMLET, respectively, whereas the LD50 of Vero was 5.7nM. The strength of the tumoricidal effect appeared to stem from the number of oleic acid molecules present. Our result suggests that LIMLET, like HAMLET, is an interesting nanolipoplex that can potentially be developed into tumor treatments. PMID:27424089

  10. Comparative distribution study of C labelled amino acids, glucose-analogue and precursor of nucleic acid, as tumor seeking agents

    Energy Technology Data Exchange (ETDEWEB)

    Shiba, Kazuhiro; Mori, Hirofumi; Hisada, Kinichi

    1984-08-01

    As tumor-seeking agents, glucose analogues, natural amino acids, synthetic nonmetabolized amino acids, and precursor of nucleic acids, etc., labeled with positron emitter, such as C and YF have been recently investigated. However, there are very few reports concerning comparative study of tumor uptake and tissue distribution of these agents. This preliminary paper describes comparative distribution and whole-body autoradiography of these agents. UC labeled deoxy-2-fluoro-D-glucose (FDG), L-, DL-leucine, 1-aminocyclopentane carboxylic acid (ACPC), -amino isobutyric acid ( -AIB), and thymidine were intravenously injected through tail vein into separate groups of the experimental animals. As the experimental animals, the mice with Ehrlich tumor and the rats with Hepatoma AH109A were used. Within 30 min after injection, FDG had the highest tumor uptake and tumor to tissue ratios, although FDG was inferior to ACPC and thymidine in related to tumor to heart, lung and brain ratios. However, the time course study indicated that tumor uptake of ACPC, -AIB and D-leucine increased with time, whereas those of other agents decreased with time or reached a plateau. Thus, at 120 min after injection, ACPC had the highest tumor uptake and tumor to tissue ratios, although ACPC was inferior to FDG in related to tumor to blood, liver and pancreas ratios. Autoradiogram of ACPC showed very clear tumor image as well as that of FDG. The above data suggest that synthetic nonmetabolized amino acids, such as ACPC may be promising as tumor-seeking agents, when used with a single photon emission computed tomography, while glucose analogue such as FDG, are the best tumor-seeking agent, when used with a positron emission computed tomography. (author).

  11. Copper(II) interactions with nonsteroidal antiinflammatory agents. I. Salicylic acid and acetylsalicylic acid.

    Science.gov (United States)

    Brumas, V; Brumas, B; Berthon, G

    1995-02-15

    Recently a growing body of evidence has accumulated on the beneficial effects of copper compounds toward various models of inflammation, and copper complexes of nonsteroidal antiinflammatory drugs (NSAIDs) have been shown to be more effective in this respect than the parent agents. However, the origin of this activity remains unclear: The ability of NSAIDs to influence copper metabolism is still questionable, and apart from the claimed SOD-like activity of copper salts in vivo, relatively little is known about how copper-NSAID interactions may help regulate the inflammatory process. Before the potential role of copper-NSAID complexes versus inflammation can be elucidated, speciation studies are necessary (i) to analyze the overall influence of these drugs on copper metabolism and (ii) to discriminate the individual complexes likely to represent the active form of the drug in vivo. In this paper, copper(II) complex equilibria with salicylic and acetylsalicylic acids--and benzoic acid used as a reference--as well as the mixed-ligand complex equilibria generated by these binary systems and L-histidine [main low-molar-mass ligand of copper(II) in blood plasma] have been investigated under physiological conditions (37 degrees C; 0.15-M NaCl). Confirming previous observations by others, resulting simulated plasma copper distributions virtually rule out any quantitative influence of salicylate on copper tissue diffusion at therapeutic levels. Even though, as is presently shown, both salicylate and acetylsalicylate may favor the gastrointestinal absorption of copper, it seems unlikely that salicylate can exert its antinflammatory activity predominantly through copper complexation. The assertion that copper-NSAID complexes represent the active forms of NSAIDs therefore seems to be of limited significance for salicylate. PMID:7876837

  12. Hypochlorous Acid as a Potential Wound Care Agent

    OpenAIRE

    Wang, L.; Bassiri, M; R. Najafi; Najafi, K.; Yang, J.; Khosrovi, B; Hwong, W; Barati, E; Belisle, B; Celeri, C; Robson, MC

    2007-01-01

    Background: A topical antimicrobial that can decrease the bacterial bioburden of chronic wounds without impairing the wound's ability to heal is a therapeutic imperative. A stabilized form of hypochlorous acid (NVC-101) has been demonstrated in vitro and in standard toxicity testing to possess properties that could fulfill these criteria. Materials and Methods: Using a standard rodent model of a chronically infected granulating wound, various preparations of NVC-101 and multiple treatment reg...

  13. Biarylalkyl Carboxylic Acid Derivatives as Novel Antischistosomal Agents.

    Science.gov (United States)

    Mäder, Patrick; Blohm, Ariane S; Quack, Thomas; Lange-Grünweller, Kerstin; Grünweller, Arnold; Hartmann, Roland K; Grevelding, Christoph G; Schlitzer, Martin

    2016-07-01

    Parasitic platyhelminths are responsible for serious infectious diseases, such as schistosomiasis, which affect humans as well as animals across vast regions of the world. The drug arsenal available for the treatment of these diseases is limited; for example, praziquantel is the only drug currently used to treat ≥240 million people each year infected with Schistosoma spp., and there is justified concern about the emergence of drug resistance. In this study, we screened biarylalkyl carboxylic acid derivatives for their antischistosomal activity against S. mansoni. These compounds showed significant influence on egg production, pairing stability, and vitality. Tegumental lesions or gut dilatation was also observed. Substitution of the terminal phenyl residue in the biaryl scaffold with a 3-hydroxy moiety and derivatization of the terminal carboxylic acid scaffold with carboxamides yielded compounds that displayed significant antischistosomal activity at concentrations as low as 10 μm with satisfying cytotoxicity values. The present study provides detailed insight into the structure-activity relationships of biarylalkyl carboxylic acid derivatives and thereby paves the way for a new drug-hit moiety for fighting schistosomiasis. PMID:27159334

  14. Plasma Sterilization of Poly Lactic Acid Ultrasound Contrast Agents: Surface Modification and Implications for Drug Delivery

    OpenAIRE

    Eisenbrey, John R.; Hsu, Jennifer; Wheatley, Margaret A.

    2009-01-01

    Poly lactic acid (PLA) ultrasound contrast agents (CA) have been previously developed in our laboratory for ultrasound (US) imaging, as well as surface coated with doxorubicin to create a potential targeted platform of chemotherapeutic delivery using focused US. However, we have previously found it impossible to sterilize these agents while at the same time maintaining their acoustic properties, a task that would probably require fabrication within a clean facility. The purpose of this paper ...

  15. Thermoresponsive Acidic Microgels as Functional Draw Agents for Forward Osmosis Desalination.

    Science.gov (United States)

    Hartanto, Yusak; Zargar, Masoumeh; Wang, Haihui; Jin, Bo; Dai, Sheng

    2016-04-19

    Thermoresponsive microgels with carboxylic acid functionalization have been recently introduced as an attractive draw agent for forward osmosis (FO) desalination, where the microgels showed promising water flux and water recovery performance. In this study, various comonomers containing different carboxylic acid and sulfonic acid functional groups were copolymerized with N-isopropylacrylamide (NP) to yield a series of functionalized thermoresponsive microgels possessing different acidic groups and hydrophobicities. The purified microgels were examined as the draw agents for FO application, and the results show the response of water flux and water recovery was significantly affected by various acidic comonomers. The thermoresponsive microgel with itaconic acid shows the best overall performance with an initial water flux of 44.8 LMH, water recovery up to 47.2% and apparent water flux of 3.1 LMH. This study shows that the incorporation of hydrophilic dicarboxylic acid functional groups into the microgels leads to the enhancement on water adsorption and overall performance. Our work elucidates in detail on the structure-property relationship of thermoresponsive microgels in their applications as FO draw agents and would be beneficial for future design and development of high performance FO desalination. PMID:27055090

  16. Esophageal Cicatricial Pemphigoid as an Isolated Involvement Treated with Mycophenolate Mofetil

    Directory of Open Access Journals (Sweden)

    Sandra Sánchez Prudencio

    2015-01-01

    Full Text Available Cicatricial pemphigoid (CP is a rare blistering autoimmune disease. Esophageal involvement occurs in widespread disease and rarely appears as the only affected organ. We report a 67-year-old Caucasian female with esophageal dysphagia and weight loss. Several oral panendoscopies showed multiple exudative ulcerations with fibrin and webs in mid- and proximal esophagus and a peeling mucosa. There were no lesions in other organs. We established the diagnosis performing a direct immunofluorescence (DIF, demonstrating IgG3 and complement deposition along the basement membrane. As initial treatment the patient received prednisone 60 mg and 1 gr twice daily of mycophenolate mofetil (MMF as a steroid-sparing agent due to its lower toxicity and its selective mechanism of action. Six months later there was a significant clinical improvement and the esophageal ulcerations had disappeared, developing cicatricial fibrous rings, although no stenosis was present. Four years later, the patient remains asymptomatic with a low maintenance dose of MMF.

  17. Mycophenolate Mofetil;A Review of Indications and Use in a Large Tertiary Hospital

    Directory of Open Access Journals (Sweden)

    Nimeshan Geevasinga

    2005-12-01

    Full Text Available Mycophenolate Mofetil (MMF has been registered for use in Australia since 1997 for prophylaxis of solid organ allograft rejection. MMF is now increasingly used for indications outside solid organ allograft rejection, often with limited supporting efficacy data. The purpose of this audit was to examine the patterns of use, reported side effects and cost impact of the drug in the Clinical and Immunology and Allergy (CIA unit of Australia’s largest teaching hospital. Prescription patterns for MMF by consultant immunologists at Westmead hospital between 2000 and 2004 were obtained from the pharmacy. These data were sorted for non-S100 indications. A single immunologist then reviewed the patient files. We also reviewed the literature on the use of this promising immunosuppressant. There has been a marked increase in use of MMF since year 2000 by the Department of CIA. A total of 75 patients were prescribed MMF for non-S100 indications. Common indications were systemic lupus erythematosus, pemphigus vulgaris, chronic idiopathic urticaria, myasthenia gravis, polymyositis, atopic dermatitis, Sjögren’s disease, uveitis and vasculitis. It is clear that MMF has potential for use in a number of immunological disorders because of its relatively benign side effect profile and observed efficacy. Double blinded, placebo-controlled, multicentre trials are necessary to establish its therapeutic role. Our study highlights some of the conditions for which this agent is useful.

  18. Pharmacokinetics and target attainment of mycophenolate in pediatric renal transplant patients.

    Science.gov (United States)

    Martial, Lisa C; Jacobs, Bart A W; Cornelissen, Elisabeth A M; de Haan, Anton F J; Koch, Birgit C P; Burger, David M; Aarnoutse, Rob E; Schreuder, Michiel F; Brüggemann, Roger J M

    2016-06-01

    MPA is an immunosuppressive agent used to prevent graft rejection after renal transplantation. MPA shows considerable inter- and intraindividual variability in exposure in children and has a defined therapeutic window, and TDM is applied to individualize therapy. We aimed to study the exposure to MPA measured as the AUC in pediatric renal transplant patients, to identify factors influencing exposure and to assess target attainment. Children transplanted between 1998 and 2014 in a single center were included. Two groups were identified: Group 1 (AUC 18 months post-transplantation). Therapeutic targets were set at: AUC0-12h of 30-60 mg h/L. A total of 39 children were included in Group 1 (median age 13.3 yr) vs. 14 in Group 2 (median age 13.4 yr). AUC0-12h was 29.7 mg h/L in Group 1 and 56.6 mg h/L in Group 2, despite a lower dosage in Group 2 (584 and 426 mg/m(2) , respectively). About 46% of patients reached the target AUC0-12h in Group 1. Time since transplantation and serum creatinine were significantly associated with MPA exposure (p explaining 36% of the variability. Individualization of the mycophenolate dose by more intense and more early TDM could improve target attainment. PMID:26923724

  19. Everolimus but not mycophenolate mofetil therapy is associated with soluble HLA-G expression in heart transplant patients

    DEFF Research Database (Denmark)

    Sheshgiri, Rohit; Gustafsson, Finn; Sheedy, Jill;

    2009-01-01

    BACKGROUND: Human leukocyte antigen-G (HLA-G), a protein primarily expressed during pregnancy, helps maintain maternal-fetal immune tolerance. Myocardial and/or soluble HLA-G (sHLA-G) expression confers protection against rejection and vasculopathy after heart transplantation. Although the precise...... mechanisms remain unclear, immunosuppressive therapy has been reported to influence this expression. METHODS: We compared sHLA-G expression in heart transplant recipients receiving two different anti-proliferative agents: mycophenolate mofetil (MMF) and everolimus (RAD). Twelve-hour pharmacokinetic (PK......-G levels and CsA exposure (R(2) = 0.43, p = 0.08). CONCLUSIONS: These preliminary findings suggest a disproportionate expression of HLA-G in patients under two distinct immunosuppression strategies after heart transplantation. Although CsA administration does not influence sHLA-G levels, RAD but not MMF is...

  20. Synthesis and evaluation of 3-acyl-tetronic acid-containing metal complexing agents

    International Nuclear Information System (INIS)

    Potential metal chelators containing one or several acyl-tetronic acid moieties were prepared from cyclic or acyclic amines and polyamines, and from bis(phenols) by reaction with 1-4 equiv of 3 bromoacetyl-tetronic acid in the presence of potassium carbonate. The affinity constants of the chelating agents for toxic metallic cations Cd2+, Cs+, and Pb2+ and for dimethylarsinic acid were measured, at pH 7.5 and 9.3. Compound 4, an acyclic triamine containing four acyl-tetronic moieties, was found to complex efficiently all the tested species. (authors)

  1. Chloramine-T as labelling agent for oleic acid and olive oil

    International Nuclear Information System (INIS)

    Olive oil and its main constituent, oleic acid, have been labelled with 125I using chloramine-T (CAT) as an oxidizing agent. The maximum yields of labelling in different organic solvents were found to vary between 10 to 50% for oleic acid. The values for olive oil were 70% of those of oleic acid. The labelled compounds were stable in organic solvents except acetone where they start to decompose after 20 minutes of starting the experiments. The low yields could be attributed partly to a possible labelling of CAT or to the reaction of CAT with labelled compounds or their precursors. (author)

  2. CJD and Scrapie Require Agent-Associated Nucleic Acids for Infection.

    Science.gov (United States)

    Botsios, Sotirios; Manuelidis, Laura

    2016-08-01

    Unlike Alzheimer's and most other neurodegenerative diseases, Transmissible Spongiform Encephalopathies (TSEs) are all caused by actively replicating infectious particles of viral size and density. Different strain-specific TSE agents cause CJD, kuru, scrapie and BSE, and all behave as latent viruses that evade adaptive immune responses and can persist for years in lymphoreticular tissues. A foreign viral structure with a nucleic acid genome best explains these TSE strains and their endemic and epidemic spread in susceptible species. Nevertheless, it is widely believed that host prion protein (PrP), without any genetic material, encodes all these strains. We developed rapid infectivity assays that allowed us to reproducibly isolate infectious particles where >85% of the starting titer separated from the majority of host components, including PrP. Remarkably, digestion of all forms of PrP did not reduce brain particle titers. To ask if TSE agents, as other viruses, require nucleic acids, we exposed high titer FU-CJD and 22L scrapie particles to potent nucleases. Both agent-strains were propagated in GT1 neuronal cells to avoid interference by complex degenerative brain changes that can impede nuclease digestions. After exposure to nucleases that are active in sarkosyl, infectivity of both agents was reproducibly reduced by ≥99%. No gold-stained host proteins or any form of PrP were visibly altered by these nucleases. In contrast, co-purifying protected mitochondrial DNA and circular SPHINX DNAs were destroyed. These findings demonstrate that TSE agents require protected genetic material to infect their hosts, and should reopen investigation of essential agent nucleic acids. J. Cell. Biochem. 117: 1947-1958, 2016. © 2016 Wiley Periodicals, Inc. PMID:26773845

  3. Effect of carboxylic acids as compatibilizer agent on mechanical properties of thermoplastic starch and polypropylene blends.

    Science.gov (United States)

    Martins, Andréa Bercini; Santana, Ruth Marlene Campomanes

    2016-01-01

    In this work, polypropylene/thermoplastic starch (PP/TPS) blends were prepared as an alternative material to use in disposable packaging, reducing the negative polymeric environmental impact. Unfortunately, this material displays morphological characteristics typical of immiscible polymer blends and a compatibilizer agent is needed. Three different carboxyl acids: myristic (C14), palmitic (C16) and stearic acids (C18) were used as natural compatibilizer agent (NCA). The effects of NCA on the mechanical, physical, thermal and morphological properties of PP/TPS blends were investigated and compared against PP/TPS with and without PP-grafted maleic anhydride (PPgMA). When compared to PP/TPS, blends with C18, PPgMA and C14 presented an improvement of 25, 22 and 17% in tensile strength at break and of 180, 194 and 259% in elongation at break, respectively. The highest increase, 54%, in the impact strength was achieved with C14 incorporation. Improvements could be seen, through scanning electron microscopy (SEM) images, in the compatibility between the immiscible components by acids incorporation. These results showed that carboxylic acids, specifically C14, could be used as compatibilizer agent and could substitute PPgMA. PMID:26453854

  4. Mycophenolate mofetil for maintenance of remission in steroid-dependent autoimmune pancreatitis

    Institute of Scientific and Technical Information of China (English)

    Jamie B Sodikoff; Steven A Keilin; Qiang cai; Sheila J Bharmal; Melinda M Lewis; Gottumukkala S Raju; Field F Willingham

    2012-01-01

    Systemic corticosteroids represent the standard treatment for autoimmune pancreatitis with IgG4-associated cholangitis.For steroid-dependent disease,azathioprine has been used for maintenance of remission.Mycophenolate mofetil has been used for transplant immunosuppression and more recently for autoimmune hepatitis; however,there are no case reports to date on the use of mycophenolate mofetil in adult patients with autoimmune pancreatitis.A patient with IgG4-mediated autoimmune pancreatitis and IgG4-associated cholangitis refractory to steroids and intolerant of azathioprine was treated with mycophenolate mofetil,which inhibits de novo guanosine synthesis and blockade of both B and T lymphocyte production.Introduction of mycophenolate mofetil and uptitration to 1000 mg by mouth twice daily over a treatment period of 4 mo was associated with improvement in the patient's energy level and blood glucose control and was not associated with any adverse events.The patient was managed without a biliary stent.However,there was a return of symptoms,jaundice,increase in transaminases,and hyperbilirubinemia when the prednisone dose reached 11 mg per day.In the first report of mycophenolate mofetil use in an adult patient with IgG4-associated autoimmune pancreatitis and IgG4-associated cholangitis,the introduction of mycophenolate mofetil was safe and well-tolerated without adverse events,but it did not enable discontinuation of the steroids.Mycophenolate mofetil and other immunomodulatory therapies should continue to be studied for maintenance of remission in the large subset of patients with refractory or recurrent autoimmune pancreatitis.

  5. Anti-AIDS agents. 30. Anti-HIV activity of oleanolic acid, pomolic acid, and structurally related triterpenoids.

    Science.gov (United States)

    Kashiwada, Y; Wang, H K; Nagao, T; Kitanaka, S; Yasuda, I; Fujioka, T; Yamagishi, T; Cosentino, L M; Kozuka, M; Okabe, H; Ikeshiro, Y; Hu, C Q; Yeh, E; Lee, K H

    1998-09-01

    Oleanolic acid (1) was identified as an anti-HIV principle from several plants, including Rosa woodsii (leaves), Prosopis glandulosa (leaves and twigs), Phoradendron juniperinum (whole plant), Syzygium claviflorum (leaves), Hyptis capitata (whole plant), and Ternstromia gymnanthera (aerial part). It inhibited HIV-1 replication in acutely infected H9 cells with an EC50 value of 1.7 microg/mL, and inhibited H9 cell growth with an IC50 value of 21.8 microg/mL [therapeutic index (T. I.) 12.8]. Pomolic acid, isolated from R. woodsii and H. capitata, was also identified as an anti-HIV agent (EC50 1.4 microg/mL, T. I. 16.6). Although ursolic acid did show anti-HIV activity (EC50 2.0 microg/mL), it was slightly toxic (IC50 6.5 microg/mL, T. I. 3.3). A new triterpene (11) was also isolated from the CHCl3-soluble fraction of R. woodsii, though it showed no anti-HIV activity. The structure of 11 was determined to be 1beta-hydroxy-2-oxopomolic acid by spectral examination. Based on these results, we examined the anti-HIV activity of oleanolic acid- or pomolic acid-related triterpenes isolated from several plants. In addition, we previously demonstrated that derivatives of betulinic acid, isolated from the leaves of S. claviflorum as an anti-HIV principle, exhibited extremely potent anti-HIV activity. Accordingly, we prepared derivatives of oleanolic acid and evaluated their anti-HIV activity. Among the oleanolic acid derivatives, 18 demonstrated most potent anti-HIV activity, with an EC50 value of 0. 0005 microg/mL and a T. I. value of 22 400. PMID:9748372

  6. 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).

  7. Lactic acid bacteria from fresh fruit and vegetables as biocontrol agents of phytopathogenic bacteria and fungi

    OpenAIRE

    Trias Mansilla, Rosalia; Bañeras Vives, Lluís; Montesinos Seguí, Emilio; Badosa Romañó, Esther

    2008-01-01

    This study evaluated the efficacy of lactic acid bacteria (LAB) isolated from fresh fruits and vegetables as biocontrol agents against the phytopathogenic and spoilage bacteria and fungi, Xanthomonas campestris, Erwinia carotovora, Penicillium expansum, Monilinia laxa, and Botrytis cinerea. The antagonistic activity of 496 LAB strains was tested in vitro and all tested microorganisms except P. expansum were inhibited by at least one isolate. The 496 isolates were also analyzed for the inhibit...

  8. Some novel antimicrobial therapeutic agents for acetylcholinesterase inhibitors; synthesis of hydroxyquinoline ester involving amino acid

    OpenAIRE

    Şakıyan, İffet; Aynacı, Elif; Arslan, Fatma; Öğütcü, Hatice; Sarı, Nurşen

    2015-01-01

    The aim of this work was to investigate the new effective agents candidate for treatment of the Alzheimer’s disease. So, a series of new and highly active acetylcholinesterase inhibitors derived from hydroxyquinoline ester containing amino acid were synthesized. Antibacterial activities of the molecules were studied by the well-diffusion method against Listeria monocytogenes 4b, Staphylococcus aureus, Escherichia coli, Salmonella typhi H, Brucella abortus, Staphylococcus epidermis sp., ...

  9. Non-chewable antacid formulations: Effect of different disintegrating agents on their acid Neutralization properties

    Directory of Open Access Journals (Sweden)

    Gadad A

    2006-01-01

    Full Text Available Aim of the present work is to develop non-chewable antacid tablets using different disintegrating agents viz., microcrystalline cellulose, sodium starch glycolate (Primogel ®, and cross-linked sodium carboxymethylcellulose (cros-car-mellose sodium ®. These agents were used alone, and in combinations, both 50% intra-granularly, and 50% extra-granularly. To cover all these variables in the formulations, seven different formulations were designed. Use of different disintegrating agents have shown varying effect on disintegration time and pattern. The disintegration time for formulation I and III did not comply with the official disintegration test in distilled water, as well as in simulated gastric fluid. All formulations, except formulation I and III, showed nearly equivalent to 30 min of Rosset-Rice time for neutralization. The graphical representation shows that when the base is available in full strength, it neutralizes the acid at a faster rate, and then the amount of base goes on reducing progressively, resulting in decrease in the rate of neutralization. Based on′t′ values, formulation II and VI show that the theoretical acid-consuming capacity, and the observed acid- consuming capacity values are almost equal.

  10. Mycophenolate mofetil in pediatric renal transplantation: A single center experience.

    LENUS (Irish Health Repository)

    Raheem, Omer A

    2011-05-01

    Raheem OA, Kamel MH, Daly PJ, Mohan P, Little DM, Awan A, Hickey DP. Mycophenolate mofetil in pediatric renal transplantation: A single center experience. Pediatr Transplantation 2011: 15:240-244. © 2009 John Wiley & Sons A\\/S. Abstract:  We assessed our long-term experience with regards to the safety and efficacy of MMF in our pediatric renal transplant population and compared it retrospectively to our previous non-MMF immunosuppressive regimen. Forty-seven pediatric renal transplants received MMF as part of their immunosuppressive protocol in the period from January 1997 till October 2006 (MMF group). A previously reported non-MMF group of 59 pediatric renal transplants was included for comparative analysis (non-MMF group). The MMF group comprised 29 boys and 18 girls, whereas the non-MMF group comprised 34 boys and 25 girls. Mean age was 11.7 and 12 yr in the MMF and non-MMF groups, respectively. The incidence of acute rejection episodes was 11 (23.4%) and 14 (24%) in the MMF and non-MMF group, respectively. Two (3.3%) grafts were lost in the non-MMF group compared with one (2.1%) in the MMF group. Twenty-one (44.68%) patients in the MMF group developed post-transplant infections compared with 12 (20.33%) in the non-MMF group (p < 0.0001). In conclusion, the use of MMF in pediatric renal transplantation was not associated with a lower rejection rate or immunological graft loss. It did, however, result in a significantly higher rate of viral infections.

  11. Protective effect of mycophenolate mofetil against nephrotoxicity and hepatotoxicity induced by tacrolimus in Wistar rats.

    Science.gov (United States)

    Ferjani, Hanen; El Arem, Amira; Bouraoui, Aicha; Achour, Abedellatif; Abid, Salwa; Bacha, Hassen; Boussema-Ayed, Imen

    2016-06-01

    Tacrolimus (TAC), a calcineurin inhibitor (CNI), is clinically used as an immunosuppressive agent in the transplant recipient; however, the use of TAC is greatly limited by its nephrotoxicity and hepatotoxicity. Mycophenolate mofetil (MMF), an inhibitor of the purine synthesis, has been used in combination with many immunosuppressive drugs such as TAC. The association TAC/MMF was used in organ transplantation to increase the efficiency and reduce acute rejection rates, but the effects of MMF on TAC-induced kidney and liver injuries are still not well investigated. The aims of this study are to explore whether MMF co-administration with TAC has a renoprotective and hepatoprotective effect against TAC-induced renal and hepatic injuries and to check the implication of oxidative stress in the MMF's possible protective effect. Our results showed that MMF (at 50 mg kg(-1) body weight (b.w.)) restored creatinine, in addition to increased AST and ALT levels by TAC (at 60 mg kg(-1) b.w.). Furthermore, MMF decreased DNA damage induced by TAC in the kidney and liver of rats as assessed by comet assay. This renoprotective and hepatoprotective effect of MMF was associated with an antioxidant effect. In fact, MMF co-treatment with TAC decreased oxidative damage induced by TAC. It reduced malondialdehyde (MDA) and protein carbonyl (PC) levels as well as catalase and superoxide dismutase (SOD) activities. We conclude that the co-administration MMF with TAC protect liver and kidney against TAC toxicity via an antioxidant process. PMID:26746208

  12. Using the Chiral Organophosphorus Derivatizing Agents for Determination of the Enantiomeric Composition of Chiral Carboxylic Acids by 31PNMR Spectroscopy

    Institute of Scientific and Technical Information of China (English)

    Chao CHE; Zhong Ning ZHANG; Gui Lan HUANG; Xin Xing WANG; Zhao Hai QIN

    2004-01-01

    The use of chiral organophosphorus derivatizing agents prepared in situ from chiral tartrate or chiral diamine for the 31PNMR determination of the enantiomeric composition of chiral carboxylic acids is described. The method is accurate, reliable and convenient.

  13. Comparison of limestone, dolomite and fly ash as pre-treatment agents for acid mine drainage

    Energy Technology Data Exchange (ETDEWEB)

    Potgieter-Vermaak, S.S.; Potgieter, J.H.; Monama, P.; Van Grieken, R. [Tshwane University of Technology, Pretoria (South Africa). Dept. of Chemistry

    2006-04-15

    The physical, chemical and biological nature of Vaal Dam water, the main source of water in Gauteng, South Africa, is often affected by underground water pollution (acid mine water) and industrial effluents. The ecological significance and detrimental effects necessitate investigations into treating the water prior to discharge into public streams. In this investigation, limestone, dolomite and fly ash were selected as pre-treatment agents based on their low cost. Simulated acid mine water containing these agents was tested using a Jar Test apparatus. Samples were analyzed before and after treatment for pH, ferrous, ferric, calcium, magnesium and sulphate ions. The study demonstrated that the quality of the water improved with an increase in the amount and surface area of the raw material dosed and an increase in contact time. It was also influenced by the chemical composition of the acid mine water and aeration. Chemical cost savings of 38% are achieved when lime is replaced with limestone, and cost savings of 23% and 48% can be accomplished when limestone is substituted with dolomite and fly ash respectively. This could result in significant savings to the gold and coal mining industries, and could lead to a mutual benefit/gain between industrialists/polluters and the public.

  14. Novel ultrasound contrast agents--Biodegradable poly(lactic acid) microcapsules

    Institute of Scientific and Technical Information of China (English)

    王身国; 崔文瑾; 李光明; 蔡晴; 智光; 赵玉英; 杨波; 徐勇

    2003-01-01

    As a novel ultrasound diagnostic contrast agent, the preparation, characterization and ultrasound imaging in the body of dog about poly(lactic acid) (PLLA) microcapsules have been studied. The behavior of this kind of contrast agent in the microcirculation was also investigated. Prepared by (water/oil/water) emulsion-solvent evaporation protocol, the PLLA microcapsules with hollow structure can enhance the ultrasound image both in vitro and in vivo, and the enduring time can last as long as 3 h. The microcirculation examination shows that the PLLA microcapsules with a diameter ranging from 2 to 8 μm could pass through the pulmonary capillaries without retention. All the results prove the PLLA microcapsules for potential use for the clinical application.

  15. Application and appreciation of chemical sand fixing agent-poly (aspartic acid) and its composites

    Energy Technology Data Exchange (ETDEWEB)

    Yang Jun; Cao Hui; Wang Fang [Beijing Key Laboratory of Bioprocess, Beijing University of Chemical Technology, Beijing 100029 (China); Tan Tianwei [Beijing Key Laboratory of Bioprocess, Beijing University of Chemical Technology, Beijing 100029 (China)], E-mail: twtan@mail.buct.edu.cn

    2007-12-15

    The sand fixing agent-poly (aspartic acid) (PASP) and its composites were applied in the field by two forms (spraying around by PASP solution and PASP powder directly). It was found that the sand fixing effect in powder form was not as good as in solution form, but it was more practical in dry region. It needed 9, 6 and 7 days for PASP, xanthan gum-PASP (X2) and ethyl cellulose-PASP (E3) to attain the maximal mechanical strength after they were applied, respectively. The sand fixing effect decreased when the material was subjected to repeated hydration-dehydration cycles and the material had no negative influence on plant growth. The PASP and its composites had water-retaining ability and could reduce the water evaporation. - The sand fixing agent was applied in powder form and it had no negative influence on plant growth.

  16. Application and appreciation of chemical sand fixing agent-poly (aspartic acid) and its composites

    International Nuclear Information System (INIS)

    The sand fixing agent-poly (aspartic acid) (PASP) and its composites were applied in the field by two forms (spraying around by PASP solution and PASP powder directly). It was found that the sand fixing effect in powder form was not as good as in solution form, but it was more practical in dry region. It needed 9, 6 and 7 days for PASP, xanthan gum-PASP (X2) and ethyl cellulose-PASP (E3) to attain the maximal mechanical strength after they were applied, respectively. The sand fixing effect decreased when the material was subjected to repeated hydration-dehydration cycles and the material had no negative influence on plant growth. The PASP and its composites had water-retaining ability and could reduce the water evaporation. - The sand fixing agent was applied in powder form and it had no negative influence on plant growth

  17. Oxalic acid as an assisting agent for the electrodialytic remediation of chromated copper arsenate treated timber waste

    DEFF Research Database (Denmark)

    Ribeiro, Alexandra B.; Mateus, Eduardo P.; Ottosen, Lisbeth M.

    1999-01-01

    The electrodialytic process is proposed as a technique for the remediation of chromated copper arsenate treated timber waste, using oxalic acid as assisting agent. The method prowed succesfull 93% Cu, 95% Cr and 99% As was removed from the timber.......The electrodialytic process is proposed as a technique for the remediation of chromated copper arsenate treated timber waste, using oxalic acid as assisting agent. The method prowed succesfull 93% Cu, 95% Cr and 99% As was removed from the timber....

  18. ELECTROLESS COPPER PLATING ON FRAXINUS MANDSHURICA VENEER USING GLYOXYLIC ACID AS REDUCING AGENT

    OpenAIRE

    Lijuan Wang; Lili Sun; Jian Li

    2011-01-01

    Copper coating was deposited on Fraxinus mandshurica veneers for preparing EMI shielding composite by electroless plating using glyoxylic acid as reducing agent in the solution. XPS and SEM were used to analyze the activation process. It was found that a continuous chitosan membrane was loaded on the wood surface. XPS results showed that Pd(II) ions were chemically adsorbed on a chitosan membrane on the wood surface through an N-Pd σ coordination bond. After reduction, part of Pd(II) absorbed...

  19. Evaluation of unnatural cyclic amino acids as boron delivery agents for treatment of melanomas and gliomas

    International Nuclear Information System (INIS)

    Unnatural cyclic amino acids (UNAAs) are a new class of boron delivery agents that are in a pre-clinical stage of evaluation. In the present study, the biodistribution of racemic forms of the cis- and trans-isomers of the boronated UNAA 1-amino-3-boronocyclopentanecarboxylic acid (ABCPC) and 1-amino-3-boronocycloheptanecarboxylic acid (ABCHC) were evaluted in B16 melanoma bearing mice and this was compared to L-p-boronophenylalanine (BPA). Boron concentrations were determined by inductively coupled plasma-optical emission spectroscopy (ICP-OES) at 2.5 h following intraperitoneal (i.p.) injection of the test agents at a concentration equivalent to 24 mg/B/kg. While all compounds attained comparable tumor boron concentrations, the tumor/blood (T/Bl) boron concentration ratios were far superior for both cis-ABCPC and cis-ABCHC compared to BPA (T/Bl=16.4, and 15.1 vs. 5.4). Secondary ion mass spectrometry (SIMS) imaging revealed that the cis-ABCPC delivered boron to the nuclei, as well as the cytoplasm of B16 cells. Next, a biodistribution study of cis-ABCPC and BPA was carried out in F98 glioma bearing rats following i.p. administration. Both compounds attained comparable tumor boron concentrations but the tumor/brain (T/Br) boron ratio was superior for cis-ABCPC compared to BPA (6 vs. 3.3). Since UNAAs are water soluble and cannot be metabolized by tumor cells, they could be potentially more effective boron delivery agents than BPA. Our data suggest that further studies are warranted to evaluate these compounds prior to the initiation of clinical studies. - Highlights: • Unnatural cyclic amino acids (UNAAs) are a new class of boron delivery agents for neutron capture therapy. • ABCPC and ABCHC attained higher tumor/blood ratios vs. BPA in B16 melanoma bearing mice. • The tumor/brain ratio of cis-ABCPC was superior to BPA (6 vs. 3.3) suggesting that further studies are warranted

  20. Mycophenolate mofetil versus azathioprine for maintenance treatment of lupus nephritis.

    Science.gov (United States)

    Kaballo, Babikir G; Ahmed, Ahmed Elias; Nur, Musa Mohammed; Khalid, Ismail Osman; Abu-Aisha, Hasan

    2016-01-01

    To compare the efficacy of mycophenolate mofetil (MMF) with that of azathioprine (AZA) drugs in the maintenance therapy of lupus nephritis (LN) patients, we studied 81 Sudanese patients with LN (32 in Class III, 34 in Class IV, and 15 in combined Class V + IV of the ISN/RPS 2003 Classification). All patients received induction therapy consisting of monthly intravenous pulse doses of cyclophosphamide (CYC) (500 mg/m 2 of body-surface area) for six months, plus three consecutive pulses of intravenous methylprednisolone 15 mg/kg/day of body weight (maximum 500 mg). Subsequently, 41 (50.6%) patients were randomized into a group that received oral MMF (22 mg/kg/day), and 40 (49.4%) patients randomized to a group that received oral AZA (2 mg/kg/day). All patients initially received oral prednisone (1 mg/kg of body weight daily) for four weeks. The baseline characteristics of the two groups were similar. Total remission rate was 75.3% (80.5% in MMF and 70% in AZA), complete remission rate of 54.3% (56.1% with MMF and 52.5% with AZA), and a partial remission rate of 21% (24.4% with MMF and 17.5% with AZA) over 29 months. During maintenance therapy, six patients died (four in the AZA group and two in the MMF group), and end-stage renal disease (ESRD) developed in five patients (three in the AZA group and two in the MMF group). During the 36-months of the study, both groups had comparable event-free survival rate for the composite end point of death or ESRD and rate of relapse-free survival. Furthermore, both groups had no significant differences in terms of frequency of hospitalization, amenorrhea, infection, nausea, and vomiting. We conclude that our study showed that short-term therapy with intravenous CYC followed by maintenance therapy with oral MMF or AZA had similar efficacy and safety for the treatment of patients with moderate to severe LN. PMID:27424688

  1. Radiosynthesis and biological evaluation of 99mTc-carboxymethylthioethyl iminodiacetic acid as renal imaging agent

    International Nuclear Information System (INIS)

    The ligand carboxymethylthioethyl iminodiacetic acid (CMT-IDA), an analogue of nitrilotriacetic acid (NTA) has been radiolabeled with technetium-99m to study its renal clearance and determine its potential as a renal tubular imaging agent. (99mTc(CO)3CMT-IDA)2- could be obtained in >98% radiochemical purity as determined by HPLC. Stability, hydrophilicity and plasma protein binding studies were carried out and were found to be comparable to that of (99mTc(CO)3NTA)2-. Biodistribution studies were carried out in normal Swiss mice at 10 min. p.i. and 2 h.p.i. The complex has shown renal clearance of (71.0±5.9)% ID at 10 min. p.i., which increased to (84.1±10.6)% at 2 h.p.i., with no major uptake in vital organs. (author)

  2. Clinical experience with mycophenolate mofetil in systemic autoimmune conditions refractory to common immunosuppressive therapies

    OpenAIRE

    Bandelier, Cédric; Guerne, Pierre-André; Genevay, Stéphane; Finckh, Axel; Gabay, Cem

    2009-01-01

    OBJECTIVES: Standard therapies against inflammatory rheumatic diseases consist of immunosuppressive drugs with high toxicities and many side effects. Except in the treatment of systemic lupus erythematosus with renal involvement, controlled studies with mycophenolate mofetil (MMF) are lacking in other autoimmune and inflammatory systemic diseases. Here we describe our clinical experience with MMF in several unusual indications. METHODS: We collected data including serological findings, advers...

  3. Calcineurin inhibitor sparing with mycophenolate in kidney transplantation: a systematic review and meta-analysis.

    LENUS (Irish Health Repository)

    Moore, Jason

    2009-02-27

    Limiting the exposure of kidney transplant recipients to calcineurin inhibitors (CNIs) has potential merit, but there is no clear consensus on the utility of current strategies. In an attempt to aid clarification, we conducted a systematic review and meta-analysis of randomized trials that assessed CNI sparing (minimization or elimination) with mycophenolate as sole adjunctive immunosuppression.

  4. Expression, protein stability and transcriptional activity of retinoic acid receptors are affected by microtubules interfering agents and all-trans retinoic acid in primary rat hepatocytes

    OpenAIRE

    2007-01-01

    Expression, protein stability and transcriptional activity of retinoic acid receptors are affected by microtubules interfering agents and all-trans retinoic acid in primary rat hepatocytes CZECH REPUBLIC (Dvorak, Zdenek) CZECH REPUBLIC Received: 2006-08-22 Revised: 2006-11-16 Accepted: 2007-01-02

  5. α-Mangostin, a Natural Agent, Enhances the Response of NRAS Mutant Melanoma to Retinoic Acid

    Science.gov (United States)

    Xia, Yun; Chen, Jing; Gong, Chongwen; Chen, Hongxiang; Sun, Jiaming

    2016-01-01

    Background The identification and use of novel compounds alone or in combination hold promise for the fight against NRAS mutant melanoma. Material/Methods We screened a kinase-specific inhibitor library through combining it with α-Mangostin in NRAS mutant melanoma cell line, and verified the enhancing effect of α-Mangostin through inhibition of the tumorigenesis pathway. Results Within the kinase inhibitors, retinoic acid showed a significant synergistic effect with α-Mangostin. α-Mangostin also can reverse the drug resistance of retinoic acid in RARa siRNA-transduced sk-mel-2 cells. Colony assay, TUNEL staining, and the expressions of several apoptosis-related genes revealed that α-Mangostin enhanced the effect of retinoic acid-induced apoptosis. The combination treatment resulted in marked induction of ROS generation and inhibition of the AKT/S6 pathway. Conclusions These results indicate that the combination of these novel natural agents with retinoid acid may be clinically effective in NRAS mutant melanoma. PMID:27104669

  6. Synthesis and screening of ursolic acid-benzylidine derivatives as potential anti-cancer agents.

    Science.gov (United States)

    Dar, Bilal Ahmad; Lone, Ali Mohd; Shah, Wajaht Amin; Qurishi, Mushtaq Ahmad

    2016-03-23

    Ursolic acid present abundantly in plant kingdom is a well-known compound with various promising biological activities including, anti-cancer, anti-inflammatory, hepatoprotective, antiallergic and anti-HIV properties. Herein, a library of ursolic acid-benzylidine derivatives have been designed and synthesized using Claisen Schmidt condensation of ursolic acid with various aromatic aldehydes in an attempt to develop potent antitumor agents. The compounds were evaluated against a panel of four human carcinoma cell lines including, A-549 (lung), MCF-7 (breast), HCT-116 (colon), THP-1 (leukemia) and a normal human epithelial cell line (FR-2). The results from MTT assay revealed that all the compounds displayed high level of antitumor activities compared with the triazole analogs (previously reported) and the parent ursolic acid. However, compound 3b, the most active derivative was subjected to mechanistic studies to understand the underlying mechanism. The results revealed that compound 3b induced apoptosis in HCT-116 cell lines, arrest cell cycle in the G1 phase, caused accumulation of cytochrome c in the cytosol and increased the expression levels of caspase-9 and caspase-3 proteins. Therefore, compound 3b induces apoptosis in HCT-116 cells through mitochondrial pathway. PMID:26854375

  7. Efficacy and safety of a conversion from the original tacrolimus and mycophenolate mofetil to the generics Tacpan® and Mowel® after liver transplantation

    Science.gov (United States)

    Vollmar, Johanna; Bellmann, Maren Christina; Darstein, Felix; Hoppe-Lotichius, Maria; Mittler, Jens; Heise, Michael; Rüttger, Bernd; Weyer, Veronika; Zimmermann, Anca; Lang, Hauke; Galle, Peter R; Zimmermann, Tim

    2015-01-01

    Background Expensive pharmaceuticals are a major reason for cost intensive health care systems. Long-term immunosuppressive therapy plays a relevant role after organ transplantation. Patents of original drugs have expired and cheaper products are available. Little data are available regarding efficacy and safety of generic immunosuppressive agents. Methods In this prospective study, 25 patients, who were clinically stable for a minimum of 2 years after liver transplantation, were converted from the original formulations of tacrolimus (TAC) and mycophenolate mofetil to the generics Tacpan® (TAP) and Mowel® (MOW). Patients were followed-up for 6 months. Results were compared retrospectively to 25 age- and sex-matched controls treated with the original brands. Results In the matched-pair analysis of TAC trough level/dose ratio, no significant difference was found between TAP/MOW and TAC/mycophenolate mofetil groups. No acute rejection occurred in either group. In total, 17 patients reported mild side effects in the TAP/MOW group. The most common side effects were gastrointestinal symptoms. Intra-individual analysis of costs revealed a considerable cost reduction in the TAP/MOW group (in median 25.03%; P<0.001). Conclusion In summary, the use of the generics TAP/MOW is effective and seems to be safe and cost-efficient in stable liver-transplantation patients. PMID:26604701

  8. A novel function for kojic acid, a secondary metabolite from Aspergillus fungi, as antileishmanial agent.

    Directory of Open Access Journals (Sweden)

    Ana Paula D Rodrigues

    Full Text Available Kojic acid (KA is a fungal metabolite used as a topical treatment skin-whitening cosmetic agent for melasma in humans; however its potential as an anti-leishmanial agent is unknown. Chemotherapy is one of the most effective treatments for Leishmaniasis. However, the drugs available are expensive, invasive, require long-term treatment and have severe side effects. Thus, the development of new effective leishmanicidal agents is a necessity. In this study we investigated the anti-leishmanial effect of KA on L. amazonensis, following in vitro and in vivo infections. KA (50 μg/mL was found to decrease the growth by 62% (IC50 34 μg/mL and 79% (IC50 27.84 μg/mL of promastigotes and amastigotes in vitro, respectively. Ultrastructural analysis of KA-treated amastigotes showed the presence of vesicles bodies into the flagellar pocket, and an intense intracellular vacuolization and swelling of the mitochondrion. During the in vitro interaction of parasites and the host cell, KA reverses the superoxide anions (O2- inhibitory mechanism promoted by parasite. In addition, 4 weeks after KA-topical formulation treatment of infected animals, a healing process was observed with a high production of collagen fibers and a decrease in parasite burden. Thus, these results demonstrated the great potential of KA as an anti-leishmanial compound.

  9. Salvianolic acid A as a multifunctional agent ameliorates doxorubicin-induced nephropathy in rats.

    Science.gov (United States)

    Fan, Hua-Ying; Yang, Ming-Yan; Qi, Dong; Zhang, Zuo-Kai; Zhu, Lin; Shang-Guan, Xiu-Xin; Liu, Ke; Xu, Hui; Che, Xin

    2015-01-01

    Nephrotic syndrome (NS) is still a therapeutic challenge. To date there is no ideal treatment. Evidence suggest that multidrug therapy has more effect than monotherapy in amelioration of renal injury. Salvianolic acid A (SAA) is the major active component of Salviae Miltiorrhizae Bunge. Previous studies have demonstrated that SAA is a multi-target agent and has various pharmacological activities. The pleiotropic properties of SAA predict its potential in the treatment of NS. The study investigated the effect of SAA on doxorubicin-induced nephropathy. The kidney function related-biochemical changes, hemorheological parameters and oxidative stress status were determined, and histological examination using light and transmission electron microcopies and western blot analysis were also performed. Results revealed that treatment with SAA alleviated histological damages, relieved proteinuria, hypoalbuminemia and hyperlipidemia, reduced oxidative stress, as well as improving hemorheology. Furthermore, SAA restored podocin expression, down-regulated the expression of NF-κB p65 and p-IκBα while up-regulating IκBα protein expression. Overall, as a multifunctional agent, SAA has a favorable renoprotection in doxorubicin-induced nephropathy. The anti-inflammation, antioxidant, amelioration of podocyte injury, improvement of hemorheology and hypolipidemic properties may constituent an important part of its therapeutic effects. All these indicate that SAA is likely to be a promising agent for NS. PMID:26194431

  10. Aquatic photodegradation of sunscreen agent p-aminobenzoic acid in the presence of dissolved organic matter.

    Science.gov (United States)

    Zhou, Lei; Ji, Yuefei; Zeng, Chao; Zhang, Ya; Wang, Zunyao; Yang, Xi

    2013-01-01

    Dissolved organic matter (DOM) is an important photosensitizer for the phototransformation of organic contaminants in sunlit natural waters. This article focuses on the photolysis kinetics and mechanism of sunscreen agent p-aminobenzoic acid (PABA) in the presence of four kinds of DOM; Suwannee River fulvic acid (SRFA), Suwannee River humic acid (SRHA), Nordic Lake fulvic acid (NOFA) and Nordic Lake humic acid (NOHA). It is evident that direct photolysis of PABA is highly pH-dependent because different species of PABA have different electrical densities on the ring system. The presence of four kinds of DOM inhibits the photolysis of PABA primarily due to their light screening effect. Meanwhile, a complex interaction involving energy transfer, triplet carbonyl group induced electron transfer, and amino acid induced proton abstraction between PABA and DOM is verified by competition kinetics experiments and density functional theory (DFT) computation. In addition, DOM-induced singlet oxygen ((1)O(2)) and hydroxyl radical (OH) are determined to play an insignificant role in PABA photolysis by competition dynamics method. Photoproducts identification using solid phase extraction-liquid chromatography-mass spectrometry (SPE-LC-MS) techniques reveals that the distribution of the photoproducts could not be affected by the addition of DOM. Two photodegradation pathways of PABA are temporarily proposed, in which the di(tri)-polymerization of intermediates are the dominant pathway whereas the oxidation of amino group to nitryl followed by hydroxylation is a minor process. Our findings reveal that direct photolysis is the dominant transformation pathway of PABA in natural sunlit waters, while the presence of DOM could evidently influence such process by light screening effect, energy transfer, electron transfer and proton abstraction mechanism. The findings in this study provide useful information for understanding of interaction between DOM and organic contaminants. PMID

  11. Lactic acid bacteria from fresh fruit and vegetables as biocontrol agents of phytopathogenic bacteria and fungi.

    Science.gov (United States)

    Trias, Rosalia; Bañeras, Lluís; Montesinos, Emilio; Badosa, Esther

    2008-12-01

    This study evaluated the efficacy of lactic acid bacteria (LAB) isolated from fresh fruits and vegetables as biocontrol agents against the phytopathogenic and spoilage bacteria and fungi, Xanthomonas campestris, Erwinia carotovora, Penicillium expansum, Monilinia laxa, and Botrytis cinerea. The antagonistic activity of 496 LAB strains was tested in vitro and all tested microorganisms except P. expansum were inhibited by at least one isolate. The 496 isolates were also analyzed for the inhibition of P. expansum infection in wounds of Golden Delicious apples. Four strains (TC97, AC318, TM319, and FF441) reduced the fungal rot diameter of the apples by 20%; only Weissella cibaria strain TM128 decreased infection levels by 50%. Cell-free supernatants of selected antagonistic bacteria were studied to determine the nature of the antimicrobial compounds produced. Organic acids were the preferred mediators of inhibition but hydrogen peroxide was also detected when strains BC48, TM128, PM141 and FF441 were tested against E. carotovora. While previous reports of antifungal activity by LAB are scarce, our results support the potential of LAB as biocontrol agents against postharvest rot. PMID:19204894

  12. Determining Multiple Responses of Pseudomonas aeruginosa PAO1 to an Antimicrobial Agent, Free Nitrous Acid.

    Science.gov (United States)

    Gao, Shu-Hong; Fan, Lu; Peng, Lai; Guo, Jianhua; Agulló-Barceló, Míriam; Yuan, Zhiguo; Bond, Philip L

    2016-05-17

    Free nitrous acid (FNA) has recently been demonstrated as an antimicrobial agent on a range of micro-organisms, especially in wastewater-treatment systems. However, the antimicrobial mechanism of FNA is largely unknown. Here, we report that the antimicrobial effects of FNA are multitargeted. The response of a model denitrifier, Pseudomnas aeruginosa PAO1 (PAO1), common in wastewater treatment, was investigated in the absence and presence of inhibitory level of FNA (0.1 mg N/L) under anaerobic denitrifying conditions. This was achieved through coupling gene expression analysis, by RNA sequencing, and with a suite of physiological analyses. Various transcripts exhibited significant changes in abundance in the presence of FNA. Respiration was likely inhibited because denitrification activity was severely depleted, and decreased transcript levels of most denitrification genes occurred. As a consequence, the tricarboxylic acid (TCA) cycle was inhibited due to the lowered cellular redox state in the FNA-exposed cultures. Meanwhile, during FNA exposure, PAO1 rerouted its carbon metabolic pathway from the TCA cycle to pyruvate fermentation with acetate as the end product as a possible survival mechanism. Additionally, protein synthesis was significantly decreased, and ribosome preservation was evident. These findings improve our understanding of PAO1 in response to FNA and contribute toward the potential application for use of FNA as an antimicrobial agent. PMID:27116299

  13. Effect of mycophenolate mofetil on the white blood cell count and the frequency of infection in systemic lupus erythematosus.

    Science.gov (United States)

    Subedi, Ananta; Magder, Laurence S; Petri, Michelle

    2015-10-01

    Leukopenia is a common manifestation of SLE. Addition of immunosuppressive therapy in a SLE patient who is already leukopenic is a clinical concern. It could worsen leukopenia, increase the risk of infection, or both. The aim of this study was to analyze the immediate effect of mycophenolate mofetil on the white blood cell count and the rate of infection in SLE patients. Two hundred and forty-four patients within the Hopkins Lupus Cohort who were newly started on mycophenolate mofetil were included in the study. The white blood cell count and interval infection history on the day mycophenolate mofetil was started were compared with the white blood cell count and interval infection history at the next visit. The study was based on 244 patients who began taking mycophenolate mofetil in the cohort. The study population included 47 % African Americans, 44 % Caucasians, and 9 % other ethnicities. There was a slight but not statistically significant increase in the white blood cell count (6.63 vs. 7.01), after starting mycophenolate mofetil. Patients with a baseline white blood cell count <3000/mm(3) did have a statistically significant increase in the white blood cell count after starting mycophenolate mofetil (2.57 vs. 5.13, P = 0.0047). We also found a statistically significant increase in the risk of bacterial infection (but not viral infection) after starting mycophenolate mofetil (4 vs. 9 %, P = 0.0036). Leukopenia does not worsen with mycophenolate mofetil. However, mycophenolate mofetil appears to slightly increase the rate of bacterial (but not viral) infection. PMID:25836768

  14. Role of tacrolimus combination therapy with mycophenolate mofetil in the prevention of organ rejection in kidney transplant patients

    Science.gov (United States)

    Dalal, P; Shah, G; Chhabra, D; Gallon, Lorenzo

    2010-01-01

    Introduction: Several new medications are now available for immunosuppression in the kidney transplant field. Tacrolimus and mycophenolate mofetil were first introduced for immunosuppression in renal transplantation in the mid 1990s. Since then, the combination of tacrolimus and mycophenolate mofetil has been evaluated in numerous clinical trials. The outcomes of these trials have varied due to differences in induction and/or maintenance therapy, drug dosing and monitoring protocols, and study design. The aim of this review is to analyze the literature critically and to provide an overview of tacrolimus and mycophenolate mofetil combination therapy in renal transplantation. PMID:21694936

  15. Natural fatty acid synthase inhibitors as potent therapeutic agents for cancers: A review.

    Science.gov (United States)

    Zhang, Jia-Sui; Lei, Jie-Ping; Wei, Guo-Qing; Chen, Hui; Ma, Chao-Ying; Jiang, He-Zhong

    2016-09-01

    Context Fatty acid synthase (FAS) is the only mammalian enzyme to catalyse the synthesis of fatty acid. The expression level of FAS is related to cancer progression, aggressiveness and metastasis. In recent years, research on natural FAS inhibitors with significant bioactivities and low side effects has increasingly become a new trend. Herein, we present recent research progress on natural fatty acid synthase inhibitors as potent therapeutic agents. Objective This paper is a mini overview of the typical natural FAS inhibitors and their possible mechanism of action in the past 10 years (2004-2014). Method The information was collected and compiled through major databases including Web of Science, PubMed, and CNKI. Results Many natural products induce cancer cells apoptosis by inhibiting FAS expression, with fewer side effects than synthetic inhibitors. Conclusion Natural FAS inhibitors are widely distributed in plants (especially in herbs and foods). Some natural products (mainly phenolics) possessing potent biological activities and stable structures are available as lead compounds to synthesise promising FAS inhibitors. PMID:26864638

  16. Facile synthesis of graphene from graphite using ascorbic acid as reducing agent

    Science.gov (United States)

    Andrijanto, Eko; Shoelarta, Shoerya; Subiyanto, Gatot; Rifki, Sadur

    2016-04-01

    Graphene has attracted a tremendous attention in recent years due to its unique properties such as mechanical, thermal, optical and electrical properties. However, a large scale production of this material is still an issue and subjected to intense research efforts. Here, we show a simple and green approach of the graphene synthesis from graphene oxide using ascorbic acid as reduction agent. A facile synthesis of graphene (rGO) through chemical oxidation of graphite into graphene oxide (GO) was described using modified Hummers method (Improved Tour Method/ITM). The ITM method does not produce toxic gas and the temperature of the oxidation is easily controlled using ice bath. The synthesized of graphene oxide was highly soluble and stable in water. The reduction of graphene oxide into graphene was performed using ascorbic acid (AA) in mild condition. The combined ITM method and green reduction using ascorbic acid open the avenue of replacing hydrazine in the reduction of graphite oxide into graphene and may be very important step for bulk production of graphene.

  17. Performance analyses of a neutralizing agent combination strategy for the production of succinic acid by Actinobacillus succinogenes ATCC 55618.

    Science.gov (United States)

    Wang, Cheng-Cheng; Zhu, Li-Wen; Li, Hong-Mei; Tang, Ya-Jie

    2012-05-01

    A neutralizing agent combination strategy was developed to enhance the succinic acid production by Actinobacillus succinogenes ATCC 55618. First, a maximal succinic acid production of 48.2 g/L was obtained at a culture pH of 7.5. Second, NaOH and KOH were screened to identify the optimal neutralizing agent for pH control. However, the production of succinic acid did not increase, and severe cell flocculation was observed due to a high concentration of metal ions when only one neutralizing agent was used to control pH. Finally, a neutralizing agent combination strategy was developed with a supply of neutralizing agents with OH(-) and carbonate. The cell flocculation was eliminated, and a maximum succinic acid production of 59.2 g/L was obtained with 5 M NaOH and 40 g/L of MgCO(3); this production was 27.9% higher than that obtained with NaOH alone. The results obtained in this study may be useful for the large-scale industrial production of succinic acid. PMID:22002101

  18. Role of tacrolimus combination therapy with mycophenolate mofetil in the prevention of organ rejection in kidney transplant patients

    Directory of Open Access Journals (Sweden)

    P Dalal

    2010-08-01

    Full Text Available P Dalal1, G Shah1, D Chhabra2, Lorenzo Gallon21Department of Medicine, Mount Sinai Hospital, Chicago; 2Feinberg School of Medicine, Northwestern University, Chicago, Illinois, USAIntroduction: Several new medications are now available for immunosuppression in the kidney transplant field. Tacrolimus and mycophenolate mofetil were first introduced for ­immunosuppression in renal transplantation in the mid 1990s. Since then, the combination of tacrolimus and mycophenolate mofetil has been evaluated in numerous clinical trials. The outcomes of these trials have varied due to differences in induction and/or maintenance therapy, drug dosing and monitoring protocols, and study design. The aim of this review is to analyze the literature critically and to provide an overview of tacrolimus and mycophenolate mofetil combination therapy in renal transplantation.Keywords: mycophenolate mofetil, tacrolimus, kidney transplantation, immunosuppression

  19. Agents that increase phosphatidic acid inhibit the LH-induced testosterone production

    DEFF Research Database (Denmark)

    Lauritzen, L.; Nielsen, L.-L.A.; Vinggaard, Anne Marie;

    1994-01-01

    for cytochrome P-450 side chain cleavage enzyme. Thus, the inhibition appears to be exerted at a point distal to cAMP-generation but before the first enzyme in the testosterone synthetic pathway. Treatment with other agents (4ß-phorbol 12-myristate 13-acetate (PMA), A23187, and sphingosine) giving rise......The results of the present study point to phosphatidic acid (PtdOH) as a possible intracellular messenger, which might be involved in local modulation of testicular testosterone production in vivo. Propranolol (27-266 µM) induced an increased level of [H]PtdOH in isolated rat Leydig cells......, prelabeled with [H]myristate, and at the same time a strong dose-dependent inhibition of the acute testosterone production stimulated by luteinizing hormone (LH). The inhibition was not bypassed by the addition of dibutyryl-cAMP but was overcome, when 22(R)-hydroxycholesterol was added as a direct substrate...

  20. Retinoic acid metabolism blocking agents (RAMBAs): a new paradigm in the treatment of hyperkeratotic disorders.

    Science.gov (United States)

    Verfaille, Christel J; Borgers, Marcel; van Steensel, Maurice A M

    2008-05-01

    Synthetic vitamin A derivatives, retinoids,have long been the mainstay of treatment for several disorders of keratinization, notably the ichthyoses and severe acne. Some forms of psoriasis also respond well. Their considerable power comes at a price. They have dose-limiting side effects and can be highly teratogenic, limiting their use in women of childbearing age.Thus, retinoids are used less often than their potential would warrant. However, the recent development of compounds that block the catabolism of endogenous vitamin A, called Retinioic Acid Metabolism Blocking Agents or RAMBAs, offers new possibilities. With these drugs, retinoid effects with less side effects and a reduction of the post-treatment teratogenicity period due to their favourable pharmacokinetic profile might be expected. In this review, we discuss how retinoids work, how they are metabolized and how RAMBAs influence this process. We also review the presently available data from clinical trials with RAMBAs. PMID:17941881

  1. Trapping of organophosphorus chemical nerve agents in water with amino acid functionalized baskets.

    Science.gov (United States)

    Ruan, Yian; Dalkiliç, Erdin; Peterson, Paul W; Pandit, Aroh; Dastan, Arif; Brown, Jason D; Polen, Shane M; Hadad, Christopher M; Badjić, Jovica D

    2014-04-01

    We prepared eleven amino-acid functionalized baskets and used (1) H NMR spectroscopy to quantify their affinity for entrapping dimethyl methylphosphonate (DMMP, 118 Å(3) ) in aqueous phosphate buffer at pH=7.0±0.1; note that DMMP guest is akin in size to chemical nerve agent sarin (132 Å(3) ). The binding interaction (Ka ) was found to vary with the size of substituent groups at the basket's rim. In particular, the degree of branching at the first carbon of each substituent had the greatest effect on the host-guest interaction, as described with the Verloop's B1 steric parameter. The branching at the remote carbons, however, did not perturb the encapsulation, which is important for guiding the design of more effective hosts and catalysts in future. PMID:24616086

  2. Plasma sterilization of poly lactic acid ultrasound contrast agents: surface modification and implications for drug delivery.

    Science.gov (United States)

    Eisenbrey, John R; Hsu, Jennifer; Wheatley, Margaret A

    2009-11-01

    Poly lactic acid (PLA) ultrasound contrast agents (CA) have been developed previously in our laboratory for ultrasound (US) imaging, as well as surface coated with doxorubicin to create a potential targeted platform of chemotherapeutic delivery using focused US. However, we have previously found it impossible to sterilize these agents while at the same time maintaining their acoustic properties, a task that would probably require fabrication within a clean facility. The purpose of this paper is to investigate the feasibility of using plasma to sterilize these CA while maintaining maximum echogenicity, a step that would greatly facilitate in vivo investigations. Effects of plasma exposure time (1, 3 and 6 min) and intensity (low-10 mA, 6.8 W; medium-15 mA, 10.5 W; and high-25 mA, 18 W) on the CAs' acoustic properties, surface morphology, zeta potential, capacity to carry chemotherapeutics and overall sterility are described. Both increases in plasma intensity and exposure time increased CA zeta potential and also significantly increased drug payload. High-intensity plasma exposure for 3 min was found to be an optimal sterilization protocol for maximal (100%) preservation of CA echogenicity. Plasma exposure resulted in sterile samples and maintained original CA enhancement of 20 dB and acoustic half-life over 75 min, while increasing CA zeta potential by 11 mV and doxorubicin loading efficiency by 10%. This study not only shows how a highly temperature- and pressure-sensitive agent can be sterilized using plasma, but also that surface modification can be used to increase surface binding of the drug. PMID:19766380

  3. "On-off" thermoresponsive coating agent containing salicylic acid applied to maize seeds for chilling tolerance.

    Directory of Open Access Journals (Sweden)

    Yajing Guan

    Full Text Available Chilling stress is an important constraint for maize seed establishment in the field. In this study, a type of "on-off" thermoresponsive coating agent containing poly (N-isopropylacrylamide-co-butylmethacrylate (Abbr. P(NIPAm-co-BMA hydrogel was developed to improve the chilling tolerance of coated maize seed. The P(NIPAm-co-BMA hydrogel was synthesized by free-radical polymerization of N-isopropylacrylamide (NIPAm and butylmethacrylate (BMA. Salicylic acid (SA was loaded in the hydrogel as the chilling resistance agent. SA-loaded P(NIPAm-co-BMA was used for seed film-coating of two maize varieties, Huang C (HC, chilling-tolerant and Mo17 (chilling-sensitive, to investigate the coated seed germination and seedling growth status under chilling stress. The results showed that the hydrogel obtained a phase transition temperature near 12°C with a NIPAM to MBA weight ratio of 1: 0.1988 (w/w. The temperature of 12°C was considered the "on-off" temperature for chilling-resistant agent release; the SA was released from the hydrogel more rapidly at external temperatures below 12°C than above 12°C. In addition, when seedlings of both maize varieties suffered a short chilling stress (5°C, higher concentrations of SA-loaded hydrogel resulted in increased germination energy, germination percentage, germination index, root length, shoot height, dry weight of roots and shoots and protective enzyme activities and a decreased malondialdehyde content in coated maize seeds compared to single SA treatments. The majority of these physiological and biochemical parameters achieved significant levels compared with the control. Therefore, SA-loaded P(NIPAm-co-BMA, a nontoxic thermoresponsive hydrogel, can be used as an effective material for chilling tolerance in film-coated maize seeds.

  4. "On-off" thermoresponsive coating agent containing salicylic acid applied to maize seeds for chilling tolerance.

    Science.gov (United States)

    Guan, Yajing; Li, Zhan; He, Fei; Huang, Yutao; Song, Wenjian; Hu, Jin

    2015-01-01

    Chilling stress is an important constraint for maize seed establishment in the field. In this study, a type of "on-off" thermoresponsive coating agent containing poly (N-isopropylacrylamide-co-butylmethacrylate) (Abbr. P(NIPAm-co-BMA)) hydrogel was developed to improve the chilling tolerance of coated maize seed. The P(NIPAm-co-BMA) hydrogel was synthesized by free-radical polymerization of N-isopropylacrylamide (NIPAm) and butylmethacrylate (BMA). Salicylic acid (SA) was loaded in the hydrogel as the chilling resistance agent. SA-loaded P(NIPAm-co-BMA) was used for seed film-coating of two maize varieties, Huang C (HC, chilling-tolerant) and Mo17 (chilling-sensitive), to investigate the coated seed germination and seedling growth status under chilling stress. The results showed that the hydrogel obtained a phase transition temperature near 12°C with a NIPAM to MBA weight ratio of 1: 0.1988 (w/w). The temperature of 12°C was considered the "on-off" temperature for chilling-resistant agent release; the SA was released from the hydrogel more rapidly at external temperatures below 12°C than above 12°C. In addition, when seedlings of both maize varieties suffered a short chilling stress (5°C), higher concentrations of SA-loaded hydrogel resulted in increased germination energy, germination percentage, germination index, root length, shoot height, dry weight of roots and shoots and protective enzyme activities and a decreased malondialdehyde content in coated maize seeds compared to single SA treatments. The majority of these physiological and biochemical parameters achieved significant levels compared with the control. Therefore, SA-loaded P(NIPAm-co-BMA), a nontoxic thermoresponsive hydrogel, can be used as an effective material for chilling tolerance in film-coated maize seeds. PMID:25807522

  5. Glycolic Acid Ethoxylate Lauryl Ether Performance as Drag Reducing Agent in Aqueous Media Flow in Pipelines

    Directory of Open Access Journals (Sweden)

    H.A. Abdul Bari

    2008-01-01

    Full Text Available In this study, Glycolic Acid Ethoxylate Lauryl Ether (GAELE anionic surfactant performance as drag reducing agent in aqueous media flow in pipelines was investigated. Testing section length L to pipe diameter D ration (L/D, addive concentration and solution flow rates were the major variables to be investigated in the present study. All the experimental study was carried in a build up experimental rig with three pipe diameters (0.0127, 0.0254 and 0.0381 m inside diameter. The experimental results showed that the (GAELE anionic can perform as a good drag reducing agent with maximum percentage drag reduction of 73% obtained in 39.37 of L/D for 600 ppm of solution. In 26.24 L/D the highest drag reduction obtained was 53% for 600 ppm of solution. The drag reduction increases corresponding with the increasing of L/D. The setup point where the effect of the drag reducer starts to take action was at Reynolds Number Re of 21000 in L/D equals to 39.37 and at Re = 30000 in 26.24 of L/D. From experimental results, it was shown that the critical wall shear stress occur at Re = 25000 in L/D = 39.37 and at Re = 35000 in L/D = 26.24.

  6. Hyaluronic acid-functionalized single-walled carbon nanotubes as tumor-targeting MRI contrast agent

    Directory of Open Access Journals (Sweden)

    Hou L

    2015-07-01

    Full Text Available Lin Hou,* Huijuan Zhang,* Yating Wang, Lili Wang, Xiaomin Yang, Zhenzhong ZhangSchool of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, People’s Republic of China*These authors contributed equally to this workAbstract: A tumor-targeting carrier, hyaluronic acid (HA-functionalized single-walled carbon nanotubes (SWCNTs, was explored to deliver magnetic resonance imaging (MRI contrast agents (CAs targeting to the tumor cells specifically. In this system, HA surface modification for SWCNTs was simply accomplished by amidation process and could make this nanomaterial highly hydrophilic. Cellular uptake was performed to evaluate the intracellular transport capabilities of HA-SWCNTs for tumor cells and the uptake rank was HA-SWCNTs> SWCNTs owing to the presence of HA, which was also evidenced by flow cytometry. The safety evaluation of this MRI CAs was investigated in vitro and in vivo. It revealed that HA-SWCNTs could stand as a biocompatible nanocarrier and gadolinium (Gd/HA-SWCNTs demonstrated almost no toxicity compared with free GdCl3. Moreover, GdCl3 bearing HA-SWCNTs could significantly increase the circulation time for MRI. Finally, to investigate the MRI contrast enhancing capabilities of Gd/HA-SWCNTs, T1-weighted MR images of tumor-bearing mice were acquired. The results suggested Gd/HA-SWCNTs had the highest tumor-targeting efficiency and T1-relaxivity enhancement, indicating HA-SWCNTs could be developed as a tumor-targeting carrier to deliver the CAs, GdCl3, for the identifiable diagnosis of tumor.Keywords: gadolinium, magnetic resonance, SWCNTs, hyaluronic acid, contrast agent

  7. Augmenting the Antifungal Activity of an Oxidizing Agent with Kojic Acid: Control of Penicillium Strains Infecting Crops

    OpenAIRE

    Kim, Jong H.; Chan, Kathleen L.

    2014-01-01

    Oxidative treatment is one of the strategies for preventing Penicillium contamination in crops/foods. The antifungal efficacy of hydrogen peroxide (H2O2; oxidant) was investigated in Penicillium strains by using kojic acid (KA) as a chemosensitizing agent, which can enhance the susceptibility of pathogens to antifungal agents. Co-application of KA with H2O2 (chemosensitization) resulted in the enhancement of antifungal activity of either compound, when compared to the independent application ...

  8. Role of tacrolimus combination therapy with mycophenolate mofetil in the prevention of organ rejection in kidney transplant patients

    OpenAIRE

    Dalal, P; Shah, G.; D Chhabra; et al.

    2010-01-01

    P Dalal1, G Shah1, D Chhabra2, Lorenzo Gallon21Department of Medicine, Mount Sinai Hospital, Chicago; 2Feinberg School of Medicine, Northwestern University, Chicago, Illinois, USAIntroduction: Several new medications are now available for immunosuppression in the kidney transplant field. Tacrolimus and mycophenolate mofetil were first introduced for ­immunosuppression in renal transplantation in the mid 1990s. Since then, the combination of tacrolimus and mycophenolate mofetil has bee...

  9. Albuminuria after renal transplantation: maintenance with sirolimus/low-dose tacrolimus vs. mycophenolate mofetil/high-dose tacrolimus.

    Science.gov (United States)

    Miles, Clifford D; Skorupa, Jill Y; Sandoz, John P; Rigley, Theodore H; Nielsen, Kathleen J; Stevens, R Brian

    2011-01-01

    Maintenance immunosuppression with sirolimus (SRL) in renal transplantation has been associated with proteinuria. We report long-term outcomes of kidney transplant recipients maintained on steroid-free regimens, either SRL with low-dose tacrolimus (SRL/L-Tac) or mycophenolate mofetil (MMF) with high-dose tacrolimus (MMF/H-Tac). We conducted a case-matched study of 50 patients receiving MMF/H-Tac, matched 1:2 with 100 patients maintained on SRL/L-Tac. All patients were induced with rabbit antithymocyte globulin followed by early steroid withdrawal. Comparisons were made of patient and graft survival, graft function, acute rejection, and albuminuria. There were no significant differences between the SRL/L-Tac and MMF/H-Tac groups for patient survival, graft survival, occurrence of acute rejection, or graft function. There was no difference in the proportion of patients with albumin/creatinine ratio (ACR) ≥300 μg/mg (19% vs. 20%), but more patients in the SRL group were receiving renin-angiotensin system blocking agents (72% vs. 53%, p = 0.04). Only flushing the donor kidney with histidine-tryptophan-ketoglutarate solution (vs. UW solution) was predictive of albuminuria. Long-term outcomes are similar at our center for kidney transplant patients receiving either SRL/L-Tac or MMF/H-Tac. Although the occurrence of albuminuria was not different, significantly more SRL-treated patients were receiving antiproteinuric medications. PMID:21077952

  10. Retinoic acid metabolism blocking agents (RAMBAs) for treatment of cancer and dermatological diseases.

    Science.gov (United States)

    Njar, Vincent C O; Gediya, Lalji; Purushottamachar, Puranik; Chopra, Pankaj; Vasaitis, Tadas Sean; Khandelwal, Aakanksha; Mehta, Jhalak; Huynh, Carlic; Belosay, Aashvini; Patel, Jyoti

    2006-07-01

    The naturally occurring retinoids and their synthetic analogs play a key role in differentiation, proliferation, and apoptosis, and their use/potential in oncology, dermatology and a variety of diseases are well documented. This review focuses on the role of all-trans-retinoic acid (ATRA), the principal endogenous metabolite of vitamin A (retinol) and its metabolism in oncology and dermatology. ATRA has been used successfully in differentiated therapy of acute promyelocytic leukemia, skin cancer, Kaposi's sarcoma, and cutaneous T-cell lymphoma, and also in the treatment of acne and psoriasis. However, its usefulness is limited by the rapid emergence of acquired ATRA resistance involving multifactoral mechanisms. A key mechanism of resistance involves ATRA-induced catabolism of ATRA. Thus, a novel strategy to overcome the limitation associated with exogenous ATRA therapy has been to modulate and/or increase the levels of endogenous ATRA by inhibiting the cytochrome P450-dependent ATRA-4-hydroxylase enzymes (particularly CYP26s) responsible for ATRA metabolism. These inhibitors are also referred to as retinoic acid metabolism blocking agents (RAMBAs). This review highlights development in the design, synthesis, and evaluation of RAMBAs. Major emphasis is given to liarozole, the most studied and only RAMBA in clinical use and also the new RAMBAs in development and with clinical potential. PMID:16530416

  11. Dynamic wettability of wood surface modified by acidic dyestuff and fixing agent

    Science.gov (United States)

    Wei, Shuangying; Shi, Junyou; Gu, Jiyou; Wang, Di; Zhang, Yanhua

    2012-01-01

    Acidic dyestuffs can bring brilliant colors to the wood and fixing agents can avoid the color loss. They could change the surface wettability of wood, which impact the gluing process of veneers. In condition of the higher moisture content of wood, the rare veneers, the veneers dyed by acidic dyestuffs and the dyed veneers fixed by Chitosan were glued respectively by one-component wet-curing isocyanate adhesive and the contact angles (θ) of the different gluing interfaces were measured. The dynamic wettability of these gluing interfaces was characterized by both the contact angle θ and the spreading-penetration parameter (K) calculated by θ. The results showed that the θ-values decreased significantly with the extension of time and the initial contact angles (θi) decreased with the moisture contents of veneers increasing, but the variation of the balance contact angles (θe) was reversed with θi. When the moisture contents of veneers were same, the variation of θ of the rare veneers was minimal and the variation of θ of the fixed veneers was maximal. The K-values of these gluing interfaces all decreased significantly with the moisture contents of veneers increasing, but the variations of K were different. The wetting model describing the dynamic wetting process was established on the basis of these variations.

  12. Amino acid esters substituted phosphorylated emtricitabine and didanosine derivatives as antiviral and anticancer agents.

    Science.gov (United States)

    Sekhar, Kuruva Chandra; Janardhan, Avilala; Kumar, Yellapu Nanda; Narasimha, Golla; Raju, Chamarthi Naga; Ghosh, S K

    2014-07-01

    Owing to the promising antiviral activity of amino acid ester-substituted phosphorylated nucleosides in the present study, a series of phosphorylated derivatives of emtricitabine and didanosine substituted with bioactive amino acid esters at P-atom were synthesized. Initially, molecular docking studies were screened to predict their molecular interactions with hemagglutinin-neuraminidase protein of Newcastle disease virus and E2 protein of human papillomavirus. The title compounds were screened for their antiviral ability against Newcastle disease virus (NDV) by their in ovo study in embryonated chicken eggs. Compounds 5g and 9c exposed well mode of interactions with HN protein and also exhibited potential growth of NDV inhibition. The remaining compounds exhibited better growth of NDV inhibition than their parent molecules, i.e., emtricitabine (FTC) and didanosine (ddI). In addition, the in vitro anticancer activity of all the title compounds were screenedagainst HeLa cell lines at 10 and 100 μg/mL concentrations. The compounds 5g and 9c showed an effective anticancer activity than that of the remaining title compounds with IC50 values of 40 and 60 μg/mL, respectively. The present in silico and in ovo antiviral and in vitro anticancer results of the title compounds are suggesting that the amino acid ester-substituted phosphorylated FTC and ddI derivatives, especially 5g and 9c, can be used as NDV inhibitors and anticancer agents for the control and management of viral diseases with cancerous condition. PMID:24789416

  13. GTP depletion synergizes the anti-proliferative activity of chemotherapeutic agents in a cell type-dependent manner

    Energy Technology Data Exchange (ETDEWEB)

    Lin, Tao; Meng, Lingjun [Center for Cancer and Stem Cell Biology, Institute of Biosciences and Technology, Texas A and M Health Science Center, Houston, TX 77030 (United States); Tsai, Robert Y.L., E-mail: rtsai@ibt.tamhsc.edu [Center for Cancer and Stem Cell Biology, Institute of Biosciences and Technology, Texas A and M Health Science Center, Houston, TX 77030 (United States)

    2011-10-22

    Highlights: {yields} Strong synergy between mycophenolic acid (MPA) and 5-FU in MDA-MB-231 cells. {yields} Cell type-dependent synergy between MPA and anti-proliferative agents. {yields} The synergy of MPA on 5-FU is recapitulated by RNA polymerase-I inhibition. {yields} The synergy of MPA on 5-FU requires the expression of nucleostemin. -- Abstract: Mycophenolic acid (MPA) depletes intracellular GTP by blocking de novo guanine nucleotide synthesis. GTP is used ubiquitously for DNA/RNA synthesis and as a signaling molecule. Here, we made a surprising discovery that the anti-proliferative activity of MPA acts synergistically with specific chemotherapeutic agents in a cell type-dependent manner. In MDA-MB-231 cells, MPA shows an extremely potent synergy with 5-FU but not with doxorubicin or etoposide. The synergy between 5-FU and MPA works most effectively against the highly tumorigenic mammary tumor cells compared to the less tumorigenic ones, and does not work in the non-breast cancer cell types that we tested, with the exception of PC3 cells. On the contrary, MPA shows the highest synergy with paclitaxel but not with 5-FU in SCC-25 cells, derived from oral squamous cell carcinomas. Mechanistically, the synergistic effect of MPA on 5-FU in MDA-MB-231 cells can be recapitulated by inhibiting the RNA polymerase-I activity and requires the expression of nucleostemin. This work reveals that the synergy between MPA and anti-proliferative agents is determined by cell type-dependent factors.

  14. Acute pancreatitis induced by mycophenolate mofetil in a kidney transplant patient

    OpenAIRE

    Einollahi Behzad; Dolatimehr Fardin

    2015-01-01

    Acute pancreatitis is a rare life-threatening complication in patients after kidney transplantation. Here we described a 56-year-old man who had received a living related kidney transplant for an end-stage renal disease. In his regular follow-up, his serum creatinine was gradually increased and he underwent an allograft biopsy, which revealed an interstitial nephritis/tubular atrophy grade II. Mycophenolate mofetil (MMF) was prescribed to control chronic allograft nephropathy. He presented wi...

  15. Gd-labeled glycol chitosan as a pH-responsive magnetic resonance imaging agent for detecting acidic tumor microenvironments

    OpenAIRE

    Nwe, Kido; Huang, Ching-Hui; Tsourkas, Andrew

    2013-01-01

    Neoplastic lesions can create a hostile tumor microenvironment with low extracellular pH. It is commonly believed that these conditions can contribute to tumor progression and resistance to therapy. We report the development and characterization of a pH-responsive magnetic resonance imaging contrast agent, for imaging the acidic tumor microenvironment. The preparation included conjugation of 1,4,7,10-Tetraazacyclododecane-1,4,7,10-tetraacetic acid 1-(2,5-dioxo-1-pyrrolidinyl) ester (DOTA-NHS)...

  16. Effects of mycophenolate mofetil on key pattern of coronary restenosis: a cascade of in vitro and ex vivo models

    Directory of Open Access Journals (Sweden)

    Baur Regine

    2005-05-01

    Full Text Available Abstract Background Mycophenolate mofetil (MMF, the prodrug of mycophenolic acid (MPA, is a rationally designed immunosuppressive drug. The current study investigates the effect of MMF on key pattern of restenosis in a cascade of in vitro and ex vivo models. Methods Part I of the study investigated in northern blot and cytoflow studies the effect of MMF (50, 100, 150, 200, 250, and 300 μg/mL on TNF-α induced expression of intercellular adhesion molecule 1 (ICAM-1 in human coronary endothelial cells (HCAEC and human coronary medial smooth muscle cells (HCMSMC. Part II of the study applied a human coronary 3D model of leukocyte attack, the 3DLA-model. HCAEC and HCMSMC were cultured on both sides of a polycarbonate filters, mimicking the internal elastic membrane. Leukocyte attack (LA was carried out by adding human monocytes (MC on the endothelial side. The effect of MMF (50 μg/mL on adhesion and chemotaxis (0.5, 1, 2, 3, 4, 6, and 24 h after LA and the effect on proliferation of co-cultured HCMSMC (24 h after LA was studied. In part III of the study a porcine coronary organ culture model of restenosis (POC-model was used. After ex vivo ballooning MMF (50 μg/mL was added to the cultures for a period of 1, 2, 3, 4, 5, 6, and 7 days. The effect on reactive cell proliferation and neointimal thickening was studied at day 7 and day 28 after ballooning. Results Expression of ICAM-1 in northern blot and cytoflow studies was neither clearly inhibited nor stimulated after administration of MMF in the clinical relevant concentration of 50 μg/mL. In the 3DLA-model 50 μg/mL of MMF caused a significant antiproliferative effect (p Conclusion Thus, the data demonstrate a significant antiproliferative effect of clinical relevant levels of MMF (50 μg/mL in the 3DLA-model. The antiproliferative effect was a direct antiproliferative effect that was not triggered via reduced expression of ICAM-1 or via an inhibition of MC-adhesion and chemotaxis. Probably due

  17. Enhancement of tumor radiation response by the antivascular agent 5,6-dimethylxanthenone-4-acetic acid

    International Nuclear Information System (INIS)

    Purpose: 5,6-dimethylxanthenone-4-acetic acid (DMXAA) selectively damages tumor vasculature and is currently in clinical trial as an antitumor agent. Its ability to induce synthesis of tumor necrosis factor (TNF), and its apparent selectivity for poorly-perfused regions in tumors, suggests it possible use in combination with radiotherapy. This investigation examines activity of DMXAA as a radiation modifier using two murine tumors. Methods and Materials: Tumor growth delay was evaluated using i.m. RIF-1 and MDAH-MCa-4 tumors irradiated in unanaesthetised, restrained mice (cobalt-60) using single dose or multiple fractions (8 x 2.5 Gy over 4 days) with DMXAA administered i.p. at various times in relation to irradiation. Results: Administration of DMXAA (80 μmol/kg, i.p.) immediately after radiation resulted in a large increase in tumor growth delay, giving a radiation dose modifying factor of 2.3 for RIF-1 and 3.9 for MDAH-MCa-4. The combination was less active when radiation was given 1-4 h after DMXAA, but was highly active 12-48 h after DMXAA. At the latter times, clamping the tumor blood supply caused a large increase in radioresistance. These studies suggest that cells surviving DMXAA are hypoxic for only a short period. DMXAA increased overall growth delay when administered daily during fractionated irradiation, giving an approximately additive response. Conclusions: The marked synergy between DMXAA and single dose ionising radiation may reflect the complementarity of these agents at the microregional level, with DMXAA preferentially killing hypoxic cells in poorly perfused regions. Despite additional hypoxia shortly after DMXAA treatment, surviving cells appear to reoxygenate quickly which makes it feasible to use DMXAA before and during fractionated radiotherapy. The combination of fractionated radiation and DMXAA appears to be less effective than for single dose radiation (possibly because of the smaller contribution of hypoxia under these conditions), but

  18. Erbium trifluoromethanesulfonate-catalyzed Friedel–Crafts acylation using aromatic carboxylic acids as acylating agents under monomode-microwave irradiation

    DEFF Research Database (Denmark)

    Tran, Phuong Hoang; Hansen, Poul Erik; Nguyen, Hai Truong;

    2015-01-01

    Erbium trifluoromethanesulfonate is found to be a good catalyst for the Friedel–Crafts acylation of arenes containing electron-donating substituents using aromatic carboxylic acids as the acylating agents under microwave irradiation. An effective, rapid and waste-free method allows the preparation...... of a wide range of aryl ketones in good yields and in short reaction times with minimum amounts of waste...

  19. Increase in complexation ability of humic acids with the addition of ligneous bulking agents during sewage sludge composting.

    Science.gov (United States)

    Xiong, Xiong; Yan-Xia, Li; Ming, Yang; Feng-Song, Zhang; Wei, Li

    2010-12-01

    Wood sawdust and maize straw were selected to co-compost sewage sludge to investigate the effects of organic bulking agents on the formation and molecular transformation of humic substances. The results showed that composting process increased humic acids (HA) while decreased fulvic acids (FA), and the wood sawdust and maize straw promoted the formation of HA by 25.6% and 16.1%, respectively. Results from fluorescence titration demonstrated that organic bulking agents also increased the binding ability of HA with the heavy metal ions, Cu(II) and Cd(II), but had little influence on that of FA. These findings indicate that organic materials especially wood sawdust may be used as bulking agents to reduce the mobility and bioavailability of toxic metals in solid waste composts. PMID:20724147

  20. Preparation of co-spray dried cushioning agent containing stearic acid for protecting pellet coatings when compressed.

    Science.gov (United States)

    Li, Xiao; Xu, De Sheng; Li, Min; Liu, Li; Heng, Paul

    2016-05-01

    This study investigated the applicability of stearic acid as a co-adjuvant in cushioning agent formulated to prevent coat damage when compressing coated pellets. The co-processed and physical blended fillers were prepared by spray drying and physically blending, respectively, with filler ingredients consisting of stearic acid, microcrystalline cellulose, fully gelatinized starch, and corn starch. Pellets containing drug were produced by coating onto non-pariels a drug layer of metformin followed by a sustained-release layer. Drug release from tablets composed of co-processed or physical blended fillers (0, 1, 5, and 10% stearic acid levels) and coated drug containing pellets were analyzed using similarity factor F2. Under the same force and the stearic acid level, co-processed fillers produced pellet containing tablets which showed higher F2 or t50 values and tensile strengths as well as lower yield pressures as compared with tablets containing physical blended fillers. It was shown that the destructive degree of pellet coating was significantly reduced after being co-processed by homogenization and the incorporation of stearic acid in the cushioning agents, as shown by the improved F2 and t50 values. In addition, disintegrate times of tablets containing co-processed agents decreased despite the hydrophobic stearic acid. In conclusion, the inclusion of stearic acid in co-processed cushioning agents was effective at protecting compacted coated pellets from compression-induced damage without compromising disintegratability. The findings could serve as a step towards resolving the technical challenges of balancing the drug release profiles, tablet tensile strength, and disintegration time of compacting coated pellets into multi-particulate-sustained release tablets. PMID:26289006

  1. In vitro cytotoxic and genotoxic effects of diphenylarsinic acid, a degradation product of chemical warfare agents

    International Nuclear Information System (INIS)

    Diphenylarsinic acid [DPAs(V)], a degradation product of diphenylcyanoarsine or diphenylchloroarsine, both of which were developed as chemical warfare agents, was investigated in terms of its capacity to induce cytotoxic effects, numerical and structural changes of chromosomes, and abnormalities of centrosome integrity and spindle organizations in conjunction with the effects of glutathione (GSH) depletion. DPAs(V) had toxic effects on cultured human hepatocarcinoma HepG2 cells at concentrations more than 0.5 mM. Depletion of GSH reduced the toxic effects of DPAs(V) as well as dimethylarsinic acid [DMAs(V)] toxicity, while toxicity by arsenite [iAs(III)] was enhanced. Exogenously added sulfhydryl (SH) compounds, such as dimercapropropane sulfonate (DMPS), GSH, and dithiothreitol (DTT), enhanced the toxic effects of DPAs(V) while they suppressed iAs(III) toxicity. DPAs(V) caused an increase in the mitotic index, and also structural and numerical changes in chromosomes in V79 Chinese hamster cells. Abnormality of centrosome integrity in mitotic V79 cells and multipolar spindles was also induced by DPAs(V) in a time- and concentration-dependent manner. These results suggested that highly toxic chemicals were generated by the interaction of DPAs(V) with SH compounds. Moreover, enhancements of toxicity by a combination of DPAs(V) and SH compounds suggested a risk in the use of SH compounds as a remedy for intoxication by diphenylarsenic compounds. Investigations on the effects of SH compounds on animals intoxicated with DPAs(V) are warranted

  2. Development of Novel Radiogallium-Labeled Bone Imaging Agents Using Oligo-Aspartic Acid Peptides as Carriers

    OpenAIRE

    Kazuma Ogawa; Atsushi Ishizaki; Kenichiro Takai; Yoji Kitamura; Tatsuto Kiwada; Kazuhiro Shiba; Akira Odani

    2013-01-01

    (68)Ga (T 1/2 = 68 min, a generator-produced nuclide) has great potential as a radionuclide for clinical positron emission tomography (PET). Because poly-glutamic and poly-aspartic acids have high affinity for hydroxyapatite, to develop new bone targeting (68)Ga-labeled bone imaging agents for PET, we used 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) as a chelating site and conjugated aspartic acid peptides of varying lengths. Subsequently, we compared Ga complexes, Ga-DOTA...

  3. Development of Novel Radiogallium-Labeled Bone Imaging Agents Using Oligo-Aspartic Acid Peptides as Carriers

    OpenAIRE

    Ogawa, Kazuma; Ishizaki, Atsushi; Takai, Kenichiro; Kitamura, Yoji; Kiwada, Tatsuto; Shiba, Kazuhiro; Odani, Akira

    2013-01-01

    68Ga (T 1/2 = 68 min, a generator-produced nuclide) has great potential as a radionuclide for clinical positron emission tomography (PET). Because poly-glutamic and poly-aspartic acids have high affinity for hydroxyapatite, to develop new bone targeting 68Ga-labeled bone imaging agents for PET, we used 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) as a chelating site and conjugated aspartic acid peptides of varying lengths. Subsequently, we compared Ga complexes, Ga-DOTA-(As...

  4. Reductive Leaching Kinetics of Low Grade Manganese Deposits in H2SO4 Solution Using Malonic Acid as Reducing Agent

    OpenAIRE

    Taysser Lasheen; S. A. Abu Elenein; Saleh, W A; A. H Orabi; D. A Ismaiel

    2014-01-01

    A leaching process was developed to extract manganese and metal values from Alloga manganese concentrate. The preferential leaching process was achieved through reductive leaching in dilute sulfuric acid medium with malonic acid as the reducing agent. Leaching parameters were optimized as 1.0 M H2SO4, 10% malonic acid in solid/liquid ratio 1:10 for 90 min at 80 C and using ore ground to – 74 µm. Under these conditions, the leaching efficiency of manganese reaches 97%, whilst iron dissolution ...

  5. Potassium fulvate as co-interpenetrating agent during graft polymerization of acrylic acid from cellulose.

    Science.gov (United States)

    Ghazy, Mohamed B M; El-Hai, Farag Abd; Mohamed, Magdy F; Essawy, Hisham A

    2016-10-01

    Grafting polymerization of acrylic acid onto cellulose in presence of potassium fulvate (KF) as a co-interpenetrating agent results enhanced water sorption compared to materials prepared similarly in its absence. The insertion of potassium fulvate (KF) did not affect the grafting process and is thought to proceed in parallel to the graft polymerization via intensive polycondensation reactions of its function groups (-COOH and OH) with COOH of the monomer and OH groups of cellulose. The combination of graft copolymerization and polycondensation reactions is assumed to produce interpenetrating network structure. Fourier transform infrared (FTIR) confirmed successful incorporation within the network structure which is an evidence for formation of interpenetrating network. The obtained structures showed homogeneous uniform surface as revealed by scanning electron microscopy (SEM). The obtained superabsorbent possessed high water absorbency 422 and 48.8g/g in distilled water and saline (0.9wt.% NaCl solution), respectively, and enhanced water retention even at elevated temperatures as revealed by thermogravimetric analysis (TGA). This could be explained by the high content of hydrophilic groups. The new superabsorbents proved to be efficient devices for controlled release of fertilizers which expands their use in agricultural applications. PMID:27370745

  6. ELECTROLESS COPPER PLATING ON FRAXINUS MANDSHURICA VENEER USING GLYOXYLIC ACID AS REDUCING AGENT

    Directory of Open Access Journals (Sweden)

    Lijuan Wang

    2011-06-01

    Full Text Available Copper coating was deposited on Fraxinus mandshurica veneers for preparing EMI shielding composite by electroless plating using glyoxylic acid as reducing agent in the solution. XPS and SEM were used to analyze the activation process. It was found that a continuous chitosan membrane was loaded on the wood surface. XPS results showed that Pd(II ions were chemically adsorbed on a chitosan membrane on the wood surface through an N-Pd σ coordination bond. After reduction, part of Pd(II absorbed formed very little Pd(0 particles on the chitosan-treated wood surface. The activated wood veneers were immersed into a plating bath in which copper film was successfully initiated. The coatings were characterized by SEM-EDS, XPS, and XRD. The metal deposition, surface resistivity, and electromagnetic shielding effectiveness were measured. The morphology of the coating was uniform, compact, and continuous. The wood grains were preserved on the plated wood veneer, which had a copper-like color and sheen. EDS, XPS, and XRD results indicated that the coating consisted of Cu0 with crystalline structure. The surface resistivity and copper deposition reached 175.14 mΩ•cm-2 and 21.66 g/m2 when the veneer was pretreated with 0.8 % chitosan for 8 min and plated for 30 min at 55 oC. The plated veneers exhibited good electromagnetic shielding effectiveness of over 60 dB in frequency ranging from10 MHz to 1.5 GHz.

  7. Salvianolic Acid B, a Potential Chemopreventive Agent, for Head and Neck Squamous Cell Cancer

    Directory of Open Access Journals (Sweden)

    Yuan Zhao

    2011-01-01

    Full Text Available Head and neck squamous cell cancer (HNSCC is one of the top ten cancers in the United States. The survival rate of HNSCC has only marginally improved over the last two decades. In addition, African-American men bear a disproportionate burden of this preventable disease. Therefore, a critical challenge of preventive health approaches is warranted. Salvianolic acid B (Sal-B isolated from Salvia miltiorrhiza Bge, which is a well-know Chinese medicines has been safely used to treat and prevent aging diseases for thousand of years. Recently, the anticancer properties of Sal-B have received more attention. Sal-B significantly inhibits or delays the growth of HNSCC in both cultured HNSCC cells and HNSCC xenograft animal models. The following anticancer mechanisms have been proposed: the inhibition of COX-2/PGE-2 pathway, the promotion of apoptosis, and the modulation of angiogenesis. In conclusion, Sal-B is a potential HNSCC chemopreventive agent working through antioxidation and anti-inflammation mechanisms.

  8. Caffeic acid: potential applications in nanotechnology as a green reducing agent for sustainable synthesis of gold nanoparticles.

    Science.gov (United States)

    Seo, Yu Seon; Cha, Song-Hyun; Yoon, Hye-Ran; Kang, Young-Hwa; Park, Youmie

    2015-04-01

    The sustainable synthesis of gold nanoparticles from gold ions was conducted with caffeic acid as a green reducing agent. The formation of gold nanoparticles was confirmed by spectroscopic and microscopic methods. Spherical nanoparticles with an average diameter of 29.99 ± 7.43 nm were observed in high- resolution transmission electron microscopy and atomic force microscopy images. The newly prepared gold nanoparticles exhibited catalytic activity toward the reduction of 4-nitrophenol to 4-aminophenol in the presence of sodium borohydride. This system enables the preparation of green catalysts using plant natural products as reducing agents, which fulfills the growing need for sustainability initiatives. PMID:25973494

  9. Research on the Interaction of Hydrogen-Bond Acidic Polymer Sensitive Sensor Materials with Chemical Warfare Agents Simulants by Inverse Gas Chromatography

    OpenAIRE

    Liu Yang; Qiang Han; Shuya Cao; Feng Huang; Molin Qin; Chenghai Guo; Mingyu Ding

    2015-01-01

    Hydrogen-bond acidic polymers are important high affinity materials sensitive to organophosphates in the chemical warfare agent sensor detection process. Interactions between the sensor sensitive materials and chemical warfare agent simulants were studied by inverse gas chromatography. Hydrogen bonded acidic polymers, i.e., BSP3, were prepared for micro-packed columns to examine the interaction. DMMP (a nerve gas simulant) and 2-CEES (a blister agent simulant) were used as probes. Chemical an...

  10. Lactic acid as a new therapeutic peeling agent in the treatment of lifa disease (frictional dermal melanosis

    Directory of Open Access Journals (Sweden)

    Khalifa E Sharquie

    2012-01-01

    Full Text Available Background: Lifa disease (frictional dermal melanosis is a common dermatological problem. Full strength lactic acid has been proved to be effective and safe peeling agent in the treatment of melasma. Objective: To assess the effectiveness and the safety of lactic acid chemical peeling in the treatment of lifa disease. Materials and Methods: This open label therapeutic trial was conducted in Department of Dermatology in Najaf and Baghdad Teaching Hospitals, from March 2007-October 2008. Full strength lactic acid (92%, pH 3.5 was used as a peeling agent. The treatment sessions were done every 2 weeks until the desired response was achieved (but not more than 6 sessions. The response to therapy was evaluated by objective and subjective methods. All patients were followed monthly for 3 months after the last treatment session. Results: 52 patients with typical clinical features of lifa disease were included. All patients were slim with prominent bones and low body mass index, and gave history of using the lifa (washing agent during bathing. The number of sessions ranged from 2-6 sessions. The pigmentation was improved in all patients as revealed by objective and subjective methods, and this response was statistically highly significant. No significant side effects were recorded in all treated patients. The improvement has been sustained without any obvious relapse throughout the follow-up period. Conclusion: Lactic acid peel is a new, non-costly mode of therapy in treating dermal melanosis in patients with lifa disease.

  11. Catalytic properties of graphene–metal nanoparticle hybrid prepared using an aromatic amino acid as the reducing agent

    International Nuclear Information System (INIS)

    An easy and single step process of making reduced graphene oxide nanosheet from graphene oxide (GO) in water medium has been demonstrated by using a naturally occurring non-proteinaceous amino acid (2,4-dihydroxy phenyl alanine, Dopa) as a new reducing agent and stabilizing agent. This amino acid has also been used to reduce the noble metal salt (AuCl3/AgNO3) to produce the corresponding noble metal nanoparticles (MNP) without using any external reducing and stabilizing agents. So, this amino acid has been used to reduce simultaneously GO to RGO and noble metal salts to produce corresponding MNP to form RGO–MNP nanohybrid system in a single step in water medium and also in absence of any external toxic reducing and stabilizing agents. Different techniques UV–Visible absorption spectroscopy, X-ray diffraction, transmission electron microscopy, atomic force microscopy and others have been used to characterize the reduction of GO to RGO, metal salts to produce corresponding MNPs and the formation of RGO–MNP nanohybrid systems. Moreover, this metal nanoparticle containing RGO–MNP nanohybrid system acts as a potential catalyst for the reduction of aromatic nitro to aromatic amino group. - Graphical abstract: This study demonstrates an easy, single step and eco-friendly method to make RGO and Au/AgNP simultaneously from respective precursors to form a RGO–Au/AgNP nanohybrid system using an aromatic amino acid (2,4-dihydroxy phenyl alanine, Dopa) as a new reducing agent as well as stabilizing agent in water medium. Highlights: ► Synthesis of reduced graphene oxide (RGO) nanosheet using an amino acid. ► The amino acid (Dopa) can reduce noble metal salt (Au3+/Ag+) to metal nanoparticle (MNP). ► Single step and eco-friendly synthesis of RGO-MNP nanohybrid using Dopa. ► Characterization of RGO, MNP and RGO–MNP nanohybrid. ► RGO-MNP nanohybrid acts as a catalyst for the reduction of aromatic nitro

  12. Pharmacokinetics of chlorogenic acid and corydaline in DA-9701, a new botanical gastroprokinetic agent, in rats.

    Science.gov (United States)

    Jung, Ji Won; Kim, Ju Myung; Jeong, Jin Seok; Son, Miwon; Lee, Hye Suk; Lee, Myung Gull; Kang, Hee Eun

    2014-07-01

    1.Few studies describing the pharmacokinetic properties of chlorogenic acid (CA) and corydaline (CRD) which are marker compounds of a new prokinetic botanical agent, DA-9701, have been reported. The aim of the present study is to evaluate the pharmacokinetic properties CA and CRD following intravenous and oral administration of pure CA (1-8 mg/kg) or CRD (1.1-4.5 mg/kg) and their equivalent dose of DA-9701 to rats. 2.  Dose-proportional AUC and dose-independent clearance (10.3-12.1 ml/min/kg) of CA were observed following its administration. Oral administration of CA as DA-9701 did not influence the oral pharmacokinetic parameters of CA. Incomplete absorption of CA, its decomposition in the gastrointestinal tract, and/or pre-systemic metabolism resulted in extremely low oral bioavailability (F) of CA (0.478-0.899%). 3.  CRD showed greater dose-normalized AUC in the higher dose group than that in lower dose group(s) after its administration due to saturation of its metabolism via decreased non-renal clearance (by 51.3%) and first-pass extraction. As a result, the F of CRD following 4.5 mg/kg oral CRD (21.1%) was considerably greater than those of the lower dose groups (9.10 and 13.8%). However, oral administration of CRD as DA-9701 showed linear pharmacokinetics as a result of increased AUC and F in lower-dose groups (by 182% and 78.5%, respectively) compared to those of pure CRD. The greater oral AUC of CRD for DA-9701 than for pure CRD could be due to decreased hepatic and/or GI first-pass extraction of CRD by other components in DA-9701. PMID:24417753

  13. Gallic Acid as a Complexing Agent for Copper Chemical Mechanical Polishing Slurries at Neutral pH

    Science.gov (United States)

    Kim, Yung Jun; Kang, Min Cheol; Kwon, Oh Joong; Kim, Jae Jeong

    2011-05-01

    Gallic acid was investigated as a new complexing agent for copper (Cu) chemical mechanical polishing slurries at neutral pH. Addition of 0.03 M gallic acid and 1.12 M H2O2 at pH 7 resulted in a Cu removal rate of 560.73±17.49 nm/min, and the ratio of the Cu removal rate to the Cu dissolution rate was 14.8. Addition of gallic acid improved the slurry performance compared to glycine addition. X-ray photoelectron spectroscopy analysis and contact angle measurements showed that addition of gallic acid enhanced the Cu polishing behavior by suppressing the formation of surface Cu oxide.

  14. New method for studying the efficiency of chelating agents of the polyamine acid series for internal decontamination

    International Nuclear Information System (INIS)

    We followed the biological fate of a complex formed on one side with either a rare earth (cerium-144) or a transuranium element (plutonium-239), and on the other side with a chelating agent of the polyamino acid series (EDTA, BAETA, DTPA, TTHA). This method allowed to study: 1 - the in vivo stability of the various complexes and to compare them; 2 - the stability of the complexes as a function of the isotope - chelating agent weight relationships; 3 - the metabolism of the chelating agents resulting in stable complexes, i. e. DTPA and TTHA mainly. This simple method brought out the higher efficiency, of DTPA in chelating rare earths and plutonium and for therapeutic purposes. (authors)

  15. Data of thermal degradation and dynamic mechanical properties of starch-glycerol based films with citric acid as crosslinking agent.

    Science.gov (United States)

    González Seligra, Paula; Medina Jaramillo, Carolina; Famá, Lucía; Goyanes, Silvia

    2016-06-01

    Interest in biodegradable edible films as packaging or coating has increased because their beneficial effects on foods. In particular, food products are highly dependents on thermal stability, integrity and transition process temperatures of the packaging. The present work describes a complete data of the thermal degradation and dynamic mechanical properties of starch-glycerol based films with citric acid (CA) as crosslinking agent described in the article titled: "Biodegradable and non-retrogradable eco-films based on starch-glycerol with citric acid as crosslinking agent" González Seligra et al. (2016) [1]. Data describes thermogravimetric and dynamical mechanical experiences and provides the figures of weight loss and loss tangent of the films as a function of the temperature. PMID:27158645

  16. Case study of the effectiveness of nitrogen foam and water-zone diverting agents in multistage matrix acid treatments

    International Nuclear Information System (INIS)

    Several oil wells producing water have been stimulated successfully with multistages of mud acid, nitrogen foam, and water-zone diverting agents. This procedure has improved well performance significantly while having little or no effect on post-treatment water production. The diverters' effectiveness was analyzed with radioactive tracers, gamma spectroscopy logs, and surface pressure equipment. Results indicate that water-ozone diverters and nitrogen foam are effective diverters when used in matrix acid stimulations. Case histories and associated data are included in this paper

  17. Effects of chelating agents on protein, oil, fatty acid amd seed mineral concentrations in soybean

    Science.gov (United States)

    Soybean seed is a major source of protein and oil for human diet. Since not much information is available on the effects of chelating agents on soybean seed composition constituents, the current study aimed to investigate the effects of various chelating agents on soybean [(Glycine max (L.) Merr.)] ...

  18. Data of thermal degradation and dynamic mechanical properties of starch–glycerol based films with citric acid as crosslinking agent

    OpenAIRE

    González Seligra, Paula; Medina Jaramillo, Carolina; Famá, Lucía; Goyanes, Silvia

    2016-01-01

    Interest in biodegradable edible films as packaging or coating has increased because their beneficial effects on foods. In particular, food products are highly dependents on thermal stability, integrity and transition process temperatures of the packaging. The present work describes a complete data of the thermal degradation and dynamic mechanical properties of starch–glycerol based films with citric acid (CA) as crosslinking agent described in the article titled: “Biodegradable and non-retro...

  19. “On-Off” Thermoresponsive Coating Agent Containing Salicylic Acid Applied to Maize Seeds for Chilling Tolerance

    OpenAIRE

    Guan, Yajing; Li, Zhan; He, Fei; Huang, Yutao; Song, Wenjian; Hu, Jin

    2015-01-01

    Chilling stress is an important constraint for maize seed establishment in the field. In this study, a type of “on-off” thermoresponsive coating agent containing poly (N-isopropylacrylamide-co-butylmethacrylate) (Abbr. P(NIPAm-co-BMA)) hydrogel was developed to improve the chilling tolerance of coated maize seed. The P(NIPAm-co-BMA) hydrogel was synthesized by free-radical polymerization of N-isopropylacrylamide (NIPAm) and butylmethacrylate (BMA). Salicylic acid (SA) was loaded in the hydrog...

  20. Synthesis And Characterization Of An Ion Imprinted Polymer For Cadmium Using Quinaldic Acid As Complexing Agent And Applying By Microwave

    OpenAIRE

    Asmawati; Abd.Wahid Wahab; Buchari; Paulina Taba

    2015-01-01

    Abstract A Cd2 Ion Imprinted Polymer Cd-IIP has been synthesized by copolymerizaton of cadmium ion quinaldic acid complexing agent 4-vynil pyridine monomer dimethyl sulfoxide solvent ethyleneglycoldimethacrylate EGDMA cross-linker and 22-azobis-isobutyronitrile AIBN initiator. Polymerization was conducted using a microwave at a temperature of 70 oC with heating times of 45 minutes. The template Cd2 was removed by leaching the template with ethanol and 4 M HCl washed by aquabidest and dried in...

  1. Active ingredients fatty acids as antibacterial agent from the brown algae Padina pavonica and Hormophysa triquetra

    Institute of Scientific and Technical Information of China (English)

    Gihan Ahmed El Shoubaky; Essam Abd El Rahman Salem

    2014-01-01

    Objective: To estimate the fatty acids content in the brown algae Padina pavonica (P. pavonica) and Hormophysa triquetra (H. triquetra) and evaluate their potential antimicrobial activity as bioactive compounds.Methods:The fatty acid compositions of the examined species were analyzed using gas chromatography-mass spectrometry. The antimicrobial activity of crude and fatty acids was assessed using the agar plug technique.Results:The fatty acids profile ranged from C8:0 to C20:4. Concentration of saturated fatty acids in P. pavonica was in the order palmitic>myristic>stearic whereas concentration of the unsaturated fatty acids was oleic acid>palmitoleic>9-cis-hexadecenoic>linoleic acid>α-linolenic>arachidonic> elaidic acid. H. triquetra contained high concentration of saturated fatty acids than those of P. pavonica which was in the order as follows: palmitic>margaric>myristic>nonadecyclic>stearic>caprylic>tridecylic>pentadecylic>lauric while the unsaturated fatty acids consisted of oleic>nonadecenoic>non adecadienoate>margaroleic. The crude and fatty acid extracts of H. triquetra and P. pavonica were biologically active on the tested pathogens. H.triquetra exhibited a larger inhibitory zone than P. pavonica. Conclusions: The brown algae P. pavonica and H. triquetra have high efficient amount of fatty acids and showed strong antibacterial activity, especially H. triquetra.

  2. Synthesis of new polyphosphonic acids, uranium extracting agents in a phosphoric medium

    International Nuclear Information System (INIS)

    Synthesis of organic phosphorus compounds for liquid-liquid extraction of traces of uranium in concentrated phosphoric acid is studied in view of industrial applications. Diphosphonic acids and monoesters and also triphosphonic acids and related compounds are synthetized. Extraction tests show a better efficiency than OPPA

  3. Non-chewable antacid formulations: Effect of different disintegrating agents on their acid Neutralization properties

    OpenAIRE

    Gadad A; Dandagi P; Mastiholimath V; Patil M; Rasal V; Dasankoppa F

    2006-01-01

    Aim of the present work is to develop non-chewable antacid tablets using different disintegrating agents viz., microcrystalline cellulose, sodium starch glycolate (Primogel ®), and cross-linked sodium carboxymethylcellulose (cros-car-mellose sodium ®). These agents were used alone, and in combinations, both 50% intra-granularly, and 50% extra-granularly. To cover all these variables in the formulations, seven different formulations were designed. Use of different d...

  4. An Analytical Model Approach for the Dissolution Kinetics of Magnesite Ore Using Ascorbic Acid as Leaching Agent

    Directory of Open Access Journals (Sweden)

    Nadeem Raza

    2013-01-01

    Full Text Available Ascorbic acid was used as leaching agent to investigate the dissolution kinetics of natural magnesite ore. The effects of various reaction parameters such as acid concentration, liquid-solid ratio, particle size, stirring speed, and temperature were determined on dissolution kinetics of the magnesite ore. It was found that the dissolution rate increased with increase in acid concentration, liquid-solid ratio, stirring speed, and temperature and decrease in the particle size of the ore. The graphical and statistical methods were applied to analyze the kinetic data, and it was evaluated that the leaching process was controlled by the chemical reaction, that is, . The activation energy of the leaching process was found to be 57.244 kJ mol−1 over the reaction temperature range from 313 to 343 K.

  5. Cleaning time and fate of phosphoric acid as conditioning agent on human dental enamel and dentin

    International Nuclear Information System (INIS)

    In this study the cleaning time and fate of phosphoric acid on human dental enamel and dentin have been investigated, using the radioactive tracer technique with 32P as an indicator of phosphorus. Twenty seconds were found to be sufficient for cleaning the enamel from phosphoric acid used for conditioning, and from formulations produced from its interaction with enamel. It was also found that dentin protection is necessary before conditioning with phosphoric acid due to the retention penetration of the latter through subsurface dentinal tubules. In addition, there seems to be an interaction between phosphoric acid and Ca(OH)2 leading to the formation of a sparingly soluble compound. (author)

  6. Genomic Phenotyping by Barcode Sequencing Broadly Distinguishes between Alkylating Agents, Oxidizing Agents, and Non-Genotoxic Agents, and Reveals a Role for Aromatic Amino Acids in Cellular Recovery after Quinone Exposure

    Science.gov (United States)

    Svensson, J. Peter; Quirós Pesudo, Laia; McRee, Siobhan K.; Adeleye, Yeyejide; Carmichael, Paul; Samson, Leona D.

    2013-01-01

    Toxicity screening of compounds provides a means to identify compounds harmful for human health and the environment. Here, we further develop the technique of genomic phenotyping to improve throughput while maintaining specificity. We exposed cells to eight different compounds that rely on different modes of action: four genotoxic alkylating (methyl methanesulfonate (MMS), N-Methyl-N-nitrosourea (MNU), N,N′-bis(2-chloroethyl)-N-nitroso-urea (BCNU), N-ethylnitrosourea (ENU)), two oxidizing (2-methylnaphthalene-1,4-dione (menadione, MEN), benzene-1,4-diol (hydroquinone, HYQ)), and two non-genotoxic (methyl carbamate (MC) and dimethyl sulfoxide (DMSO)) compounds. A library of S. cerevisiae 4,852 deletion strains, each identifiable by a unique genetic ‘barcode’, were grown in competition; at different time points the ratio between the strains was assessed by quantitative high throughput ‘barcode’ sequencing. The method was validated by comparison to previous genomic phenotyping studies and 90% of the strains identified as MMS-sensitive here were also identified as MMS-sensitive in a much lower throughput solid agar screen. The data provide profiles of proteins and pathways needed for recovery after both genotoxic and non-genotoxic compounds. In addition, a novel role for aromatic amino acids in the recovery after treatment with oxidizing agents was suggested. The role of aromatic acids was further validated; the quinone subgroup of oxidizing agents were extremely toxic in cells where tryptophan biosynthesis was compromised. PMID:24040048

  7. Composition dependence of the synergistic effect of nucleating agent and plasticizer in poly(lactic acid: A Mixture Design study

    Directory of Open Access Journals (Sweden)

    M. K. Fehri

    2016-04-01

    Full Text Available Blends consisting of commercial poly(lactic acid (PLA, poly(lactic acid oligomer (OLA8 as plasticizer and a sulfonic salt of a phthalic ester and poly(D-lactic acid as nucleating agents were prepared by melt extrusion, following a Mixture Design approach, in order to systematically study mechanical and thermal properties as a function of composition. The full investigation was carried out by differential scanning calorimetry (DSC, dynamic mechanical thermal analysis (DMTA and tensile tests. The crystallization half-time was also studied at 105 °C as a function of the blends composition. A range of compositions in which the plasticizer and the nucleation agent minimized the crystallization half-time in a synergistic way was clearly identified thanks to the application of the Mixture Design approach. The results allowed also the identification of a composition range to maximize the crystallinity developed during the rapid cooling below glass transition temperature in injection moulding, thus allowing an easier processing of PLA based materials. Moreover the mechanical properties were discussed by correlating them to the chemical structural features and thermal behaviour of blends.

  8. The effect of bulking agents on the chemical stability of acid-sensitive compounds in freeze-dried formulations: sucrose inversion study.

    Science.gov (United States)

    Lu, Enxian; Ewing, Susan; Gatlin, Larry; Suryanarayanan, Raj; Shalaev, Evgenyi

    2009-09-01

    The goal of the study was to evaluate the impact of amorphous bulking agents on the chemical stability of freeze-dried materials. Polyvinylpyrrolidone and dextran of different molecular weights and lactose were used as bulking agents, and sucrose was used as an example of an acid-sensitive compound. Lyophiles containing bulking agent and sucrose at 10:1 (w/w) ratio, citrate buffer, and optionally bromophenol blue (pH indicator) were tested by X-ray powder diffractometry, differential scanning calorimetry, and Karl Fischer titrimetry. Diffuse reflectance UV-vis spectroscopy was used to obtain the concentration ratio of the deprotonated (In(2-)) to the protonated (HIn(-)) indicator species, from which the Hammett acidity function (H(2-)) was calculated. The extent of sucrose inversion in lyophiles stored at 60 degrees C was quantified by HPLC. The bulking agent had a major impact on both the apparent solid-state acidity (H(2-)) and the degradation rate, with the degradation rate constants value highest for dextran lyophiles (most "acidic", lower H(2-)) followed by lactose and polyvinylpyrrolidone lyophile (least "acidic", higher H(2-)). The Hammett acidity function can be used as an empirical solid-state acidity scale, to predict the rank-order stability of acid-sensitive compounds in lyophiles prepared with different bulking agents. PMID:19544366

  9. Synthesis, characterization and application of a novel chemical sand-fixing agent-poly(aspartic acid) and its composites

    Energy Technology Data Exchange (ETDEWEB)

    Yang Jun [Beijing Key Laboratory of Bioprocess, Beijing University of Chemical Technology, Beijing 100029 (China); Wang Fang [Beijing Key Laboratory of Bioprocess, Beijing University of Chemical Technology, Beijing 100029 (China); Fang Li [Beijing Key Laboratory of Bioprocess, Beijing University of Chemical Technology, Beijing 100029 (China); Tan Tianwei [Beijing Key Laboratory of Bioprocess, Beijing University of Chemical Technology, Beijing 100029 (China)]. E-mail: twtan@mail.buct.edu.cn

    2007-09-15

    A novel sand-fixing agent-poly(aspartic acid) and its composites were synthesized to improve sand particles compressive strength and anti-wind erosion properties. The relationship between the concentration of sand-fixing agent and the sand-fixing properties was studied by three kinds of aging tests. Some composites were choose to improve the sand-fixing property and the composition of 40% xanthan gum and 60% ethyl cellulose were chosen to compare sand-fixing property with lignosulfonate. The results showed that the sand-fixing and water-retaining properties of xanthan gum and ethyl cellulose composites were better than that of lignosulfonate. The biodegradability experiment showed that the PASP and its composites were environment-friendly products and the field test showed that the PASP composites could improve wind erosion disturbance. - A novel biodegradability polymer significantly improved sand particles' compressive strength and anti-wind erosion properties.

  10. Synthesis, characterization and application of a novel chemical sand-fixing agent-poly(aspartic acid) and its composites

    International Nuclear Information System (INIS)

    A novel sand-fixing agent-poly(aspartic acid) and its composites were synthesized to improve sand particles compressive strength and anti-wind erosion properties. The relationship between the concentration of sand-fixing agent and the sand-fixing properties was studied by three kinds of aging tests. Some composites were choose to improve the sand-fixing property and the composition of 40% xanthan gum and 60% ethyl cellulose were chosen to compare sand-fixing property with lignosulfonate. The results showed that the sand-fixing and water-retaining properties of xanthan gum and ethyl cellulose composites were better than that of lignosulfonate. The biodegradability experiment showed that the PASP and its composites were environment-friendly products and the field test showed that the PASP composites could improve wind erosion disturbance. - A novel biodegradability polymer significantly improved sand particles' compressive strength and anti-wind erosion properties

  11. In vitro activity of cefmetazole, cefotetan, amoxicillin-clavulanic acid, and other antimicrobial agents against anaerobic bacteria from endometrial cultures of women with pelvic infections.

    OpenAIRE

    Ohm-Smith, M J; Sweet, R. L.

    1987-01-01

    The MICs of the new antimicrobial agents cefmetazole, cefotetan, and amoxicillin-clauvulanic acid were compared with the MICs of other antimicrobial agents against anaerobic bacteria from endometrial cultures from women with pelvic inflammatory disease or endometritis. The activity of cefmetazole was similar to that of cefoxitin and generally greater than that of cefotetan. Amoxicillin-clavulanic acid was generally more active than all cephamycins tested.

  12. Enteric-coated tablet of risedronate sodium in combination with phytic acid, a natural chelating agent, for improved oral bioavailability.

    Science.gov (United States)

    Kim, Jeong S; Jang, Sun W; Son, Miwon; Kim, Byoung M; Kang, Myung J

    2016-01-20

    The oral bioavailability (BA) of risedronate sodium (RS), an antiresorptive agent, is less than 1% due to its low membrane permeability as well as the formation of non-absorbable complexes with multivalent cations such as calcium ion (Ca(2+)) in the gastrointestinal tract. In the present study, to increase oral BA of the bisphosphonate, a novel enteric-coated tablet (ECT) dosage form of RS in combination with phytic acid (IP6), a natural chelating agent recognized as safe, was formulated. The chelating behavior of IP6 against Ca(2+), including a stability constant for complex formulation was characterized using the continuous variation method. Subsequently, in vitro dissolution profile and in vivo pharmacokinetic profile of the novel ECT were evaluated comparatively with that of the marketed product (Altevia, Sanofi, US), an ECT containing ethylenediaminetetraacetic acid (EDTA) as a chelating agent, in beagle dogs. The logarithm of stability constant for Ca(2+)-IP6 complex, an equilibrium constant approximating the strength of the interaction between two chemicals to form complex, was 19.05, which was 3.9-fold (p<0.05) and 1.7-fold (p<0.05) higher than those of Ca(2+)-RS and Ca(2+)-EDTA complexes. The release profile of RS from both enteric-coated dosage forms was equivalent, regardless of the type of chelating agent. An in vivo absorption study in beagle dogs revealed that the maximum plasma concentration and area under the curve of RS after oral administration of IP6-containing ECT were approximately 7.9- (p<0.05) and 5.0-fold (p<0.05) higher than those of the marketed product at the same dose (35mg as RS). Therefore, our study demonstrates the potential usefulness of the ECT system in combination with IP6 for an oral therapy with the bisphosphonate for improved BA. PMID:26594027

  13. Synthesis and antitussive evaluation of verticinone-cholic acid salt, a novel and potential cough therapeutic agent

    Institute of Scientific and Technical Information of China (English)

    Fang-zhou XU; Chang CHEN; Yong-hui ZHANG; Han-li RUAN; Hui-fang PI; Pong ZHANG; Ji-zhou WU

    2007-01-01

    Aim: To seek a novel and potent antitussive drug based on Shedan-Chuanbei powder, a complex of traditional Chinese medicine preparation for cough therapy.Methods: Verticinone-cholic acid (Vet-CA) salt, a novel, salifying derivative of verticinone and cholic acid, both of which are the major bioactive components in Shedan-Chuanbei powder, was synthesized. We then evaluated the antitussive activity and the acute toxicity of the salt. Results: The new compound, with good solubility in water, has much more potent antitussive activity in comparison with the same dose of single verticinone and single cholic acid. The administration 3 mg/kg of Ver-CA could result in over 50% reduction of a citric acid-induced cough.Pretreatment with naloxone (0.8 mg/kg, ip) can only partially antagonize its anti-tussive effect. On the other hand, glybenclamide (3 mg/kg, ip), an ATP-sensitive K+ channel blocker, can also significantly reduce the antitussive effect of Ver-CA.A further acute toxicity study showed that the LD50 values of Ver-CA were 3 times that of verticinone. Conclusion: Based on the studies of pharmacology and acutetoxicity, the salt has a synergic and attenuated toxicity compared with single verticinone and cholic acid. Moreover, the present study also suggests that Ver-CA, a potential novel antitussive agent, may exert its antitussive effect via both the peripheral (modulated by ATP-sensitive K+ channels) and central mechanisms(modulated by the opioid receptor).

  14. Molecular Identification of Lactic Acid Bacteria Producing Antimicrobial Agents from Bakasang, An Indonesian Traditional Fermented Fish Product

    Directory of Open Access Journals (Sweden)

    Helen Joan Lawalata

    2015-11-01

    Full Text Available AbstractTwenty seven strains of lactic acid bacteria (LAB were isolated from bakasang, Indonesian traditional fermented fish product. In general, LAB have inhibitory activity againts pathogenic bacteria and spoilage bacteria. Screening for antimicrobia activity of isolates were performed with well-diffusion method. One isolate that was designed as Pediococcus BksC24 was the strongest against bacteria pathogenic and spoilage bacteria. This strain was further identified by 16S rRNA gen sequence comparison. Isolates LAB producing antimicrobial agents from bakasang were identified as Pediococcus acidilactici.Keywords : Bakasang, LAB, antimicrobial, phenotypic characteristics, 16S rRNA gene

  15. CORRELATION OF CONTENT ASCORBIC ACID IN THE ASSIMILATION APPARATUS BETULA PENDULA ROTH. WITH AGENT BY PATHOLOGICAL

    Directory of Open Access Journals (Sweden)

    Михаил Эдуардович Баландайкин

    2014-09-01

    Full Text Available Features of influence of set of anthropogenic factors and phytopathologic state of tree Betula pendula on concentration of ascorbic acid in it assimilation apparatus are considered. By criterion of influence Inonotus obliquus (Pers.: Fr. Pilat and to presence pollution adaptable ability of a plant to action stressful factors, and also possibility of development of the mechanisms which are responsible for inhibition of biosynthesis of ascorbic acid estimated. It is shown that from all analysed in the yielded work abiotic and biotic factors most essentially the pathogenic factor affects change of concentration of ascorbic acid in sheet plates of trees concerning norm.

  16. n-octylphenylphosphonic acid as an extraction agent for scandium and hafnium

    International Nuclear Information System (INIS)

    The extraction of Sc complexes with n-octylphenylphosphonic acid (HA) from HCl, HClO4, HNO3 and H2SO4 into benzene was studied and the effect of some tri-n-alkylphosphine oxides added was investigated. Scandium was extracted into the organic phase as a ScA3(HA) complex from 2M mineral acids; when concentrated mineral acids, except for HNO3, were employed, the extraction mechanism changes and ScX3(HA)sub(n) or Sc2(SO4)3(HA)sub(n) complexes, where X was a mineral acid residue, were extracted into the organic phase. The corresponding extraction constants were determined. The substances added did not cause synergic extraction. The extraction of Hf from nitrate and sulphate media was studied analogically; with the former medium, only the solvation-mechanism extraction was observed. The IR and NMR spectra of the reagent were studied. (author)

  17. Data of thermal degradation and dynamic mechanical properties of starch–glycerol based films with citric acid as crosslinking agent

    Science.gov (United States)

    González Seligra, Paula; Medina Jaramillo, Carolina; Famá, Lucía; Goyanes, Silvia

    2016-01-01

    Interest in biodegradable edible films as packaging or coating has increased because their beneficial effects on foods. In particular, food products are highly dependents on thermal stability, integrity and transition process temperatures of the packaging. The present work describes a complete data of the thermal degradation and dynamic mechanical properties of starch–glycerol based films with citric acid (CA) as crosslinking agent described in the article titled: “Biodegradable and non-retrogradable eco-films based on starch–glycerol with citric acid as crosslinking agent” González Seligra et al. (2016) [1]. Data describes thermogravimetric and dynamical mechanical experiences and provides the figures of weight loss and loss tangent of the films as a function of the temperature. PMID:27158645

  18. CORRELATION OF CONTENT ASCORBIC ACID IN THE ASSIMILATION APPARATUS BETULA PENDULA ROTH. WITH AGENT BY PATHOLOGICAL

    OpenAIRE

    Михаил Эдуардович Баландайкин

    2014-01-01

    Features of influence of set of anthropogenic factors and phytopathologic state of tree Betula pendula on concentration of ascorbic acid in it assimilation apparatus are considered. By criterion of influence Inonotus obliquus (Pers.: Fr.) Pilat and to presence pollution adaptable ability of a plant to action stressful factors, and also possibility of development of the mechanisms which are responsible for inhibition of biosynthesis of ascorbic acid estimated. It is shown that from all analyse...

  19. Research on the Interaction of Hydrogen-Bond Acidic Polymer Sensitive Sensor Materials with Chemical Warfare Agents Simulants by Inverse Gas Chromatography

    Directory of Open Access Journals (Sweden)

    Liu Yang

    2015-06-01

    Full Text Available Hydrogen-bond acidic polymers are important high affinity materials sensitive to organophosphates in the chemical warfare agent sensor detection process. Interactions between the sensor sensitive materials and chemical warfare agent simulants were studied by inverse gas chromatography. Hydrogen bonded acidic polymers, i.e., BSP3, were prepared for micro-packed columns to examine the interaction. DMMP (a nerve gas simulant and 2-CEES (a blister agent simulant were used as probes. Chemical and physical parameters such as heats of absorption and Henry constants of the polymers to DMMP and 2-CEES were determined by inverse gas chromatography. Details concerning absorption performance are also discussed in this paper.

  20. Research on the interaction of hydrogen-bond acidic polymer sensitive sensor materials with chemical warfare agents simulants by inverse gas chromatography.

    Science.gov (United States)

    Yang, Liu; Han, Qiang; Cao, Shuya; Huang, Feng; Qin, Molin; Guo, Chenghai; Ding, Mingyu

    2015-01-01

    Hydrogen-bond acidic polymers are important high affinity materials sensitive to organophosphates in the chemical warfare agent sensor detection process. Interactions between the sensor sensitive materials and chemical warfare agent simulants were studied by inverse gas chromatography. Hydrogen bonded acidic polymers, i.e., BSP3, were prepared for micro-packed columns to examine the interaction. DMMP (a nerve gas simulant) and 2-CEES (a blister agent simulant) were used as probes. Chemical and physical parameters such as heats of absorption and Henry constants of the polymers to DMMP and 2-CEES were determined by inverse gas chromatography. Details concerning absorption performance are also discussed in this paper. PMID:26043177

  1. Regeneration of three-way automobile catalysts using biodegradable metal chelating agent-S, S-ethylenediamine disuccinic acid (S, S-EDDS)

    International Nuclear Information System (INIS)

    Regeneration of the activity of three-way catalytic converters (TWCs) was tested for the first time using a biodegradable metal chelating agent (S, S-ethylenediamine disuccinic acid (S, S-EDDS). The efficiency of this novel environmentally friendly solvent in removing various contaminants such as P, Zn, Pb, Cu and S from commercial aged three-way catalysts, and improving their catalytic performance towards CO and NO pollutants removal has been investigated. Four samples of catalysts from the front and rear inlets of two different TWCs with different mileages and aged under completely different driving conditions were investigated. The catalysts were characterized using various techniques, such as X-ray diffraction (XRD), Scanning electron microscopy (SEM), and Brunauer-Emmett-Teller (BET) surface area measurements (N2 adsorption at 77 K). Quantitative ICP-MS analyses and SEM-EDS studies show the removal of Zn, P and Pb. SEM-EDS images obtained at low magnification (50 μm) showed considerable differences in the surface morphology and composition after washing with S, S-EDDS. However, XRD studies indicated neither little to no removal of major contaminant compound phases nor major structural changes due to washing. Correspondingly, little or no enhancement in BET surface area was observed between the used and washed samples. Light-off curves show that the regeneration procedure employed can effectively improve the catalytic performance towards NO pollutant.

  2. The fatty acid synthase inhibitor triclosan: repurposing an anti-microbial agent for targeting prostate cancer

    OpenAIRE

    Sadowski, Martin C.; Pouwer, Rebecca H.; Jennifer H. Gunter; Lubik, Amy A.; Quinn, Ronald J.; Nelson, Colleen C.

    2014-01-01

    Inhibition of FASN has emerged as a promising therapeutic target in cancer, and numerous inhibitors have been investigated. However, severe pharmacological limitations have challenged their clinical testing. The synthetic FASN inhibitor triclosan, which was initially developed as a topical antibacterial agent, is merely affected by these pharmacological limitations. Yet, little is known about its mechanism in inhibiting the growth of cancer cells. Here we compared the cellular and molecular e...

  3. Synthesis and characterization of a new retinoic acid ECPIRM as potential chemotherapeutic agent for human cutaneous squamous carcinoma.

    Science.gov (United States)

    Zhang, Mengli; Tao, Yue; Ma, Pengcheng; Wang, Dechuan; He, Chundi; Cao, Yuping; Wei, Jun; Li, Lingjun; Tao, Lei

    2015-01-01

    Cutaneous squamous cell carcinoma (CSCC) is one of the most common cancers worldwide, requiring effective therapeutic interventions. Retinoids are important chemopreventive and therapeutic agents for a variety of human cancers including CSCC. In this study we synthesized a novel retinoic derivative N-(4-ethoxycarbonylphenyl) isoretinamide (ECPIRM) and evaluated its biological activities and possible mechanisms in human cutaneous squamous cell lines. ECPIRM had better inhibitory effect on the proliferation of squamous carcinoma cells SCL-1 and colo-16, compared with All-trans retinoic acid and 13-cis retinoic acid. ECPIRM had less toxicity to normal keratinocyte cell line HaCaT. Mechanistically, ECPIRM induced G1 cell cycle arrest in SCL-1 cells, via the downregulation of CDK2, CDK4, cycling D1 and cyclin E expression and upregulation of p21. In addition, these effects were at least partially due to the inhibition of JNK/ ERK-AP-1 signaling pathway by ECPIRM. Importantly, these effects of ECPIRM are independent of the classical retinoid receptor pathway, suggesting that the novel compound will have less side-effects in chemotherapy. These findings demonstrate that ECPIRM is a potential inhibitor of MPAK-AP-1 pathway, and is a potential therapeutic agent against CSCC. PMID:25991427

  4. 5-aminosalicylic acid is an attractive candidate agent for chemoprevention of colon cancer in patients with inflammatory bowel disease

    Institute of Scientific and Technical Information of China (English)

    Yang Cheng; Pierre Desreumaux

    2005-01-01

    Inflammatory bowel disease (IBD) is classically subdivided into ulcerative colitis (UC) and Crohn's disease (CD). Patients with IBD have increased risk for colorectal cancer. Because the pathogenesis of colorectal carcinoma has not been entirely defined yet and there is no ideal treatment for colon cancer, cancer prevention has become increasingly important in patients with IBD. The two adopted methods to prevent the development of colon cancer in clinical practice include the prophylactic colectomy and colonoscopic surveillance.But patients and physicians seldom accept colectomy as a routine preventive method and most patients do not undergo appropriate colonoscopic surveillance. Chemoprevention refers to the use of natural or synthetic chemical agents to reverse, suppress, or to delay the process of carcinogenesis.Chemoprevention is a particularly useful method in the management of patients at high risk for the development of specific cancers based on inborn genetic susceptibility, the presence of cancer-associated disease, or other known risk factors. Prevention of colorectal cancer by administration of chemopreventive agents is one of the most promising options for IBD patients who are at increased risks of the disease. The chemopreventive efficacy of nonsteroidal antiinflammatory drugs (NSAIDs) against intestinal tumors has been well established. But with reports that NSAIDs aggravated the symptoms of colitis, their sustained use for the purpose of cancer chemoprevention has been relatively contraindicated in IBD patients. Another hopeful candidate chemoprevention drug for IBD patients is 5-aminosalicylic acid (5-ASA), which is well tolerated by most patients and has limited systemic adverse effects, and no gastrointestinal toxicity. 5-ASA lacks the well-known side effects of longterm NSAIDs use. Retrospective correlative studies have suggested that the long-term use of 5-ASA in IBD patients may significantly reduce the risk of development of colorectal cancer

  5. Topological estimation of proton-ligand formation constants of potential antitumour agents: Salicylhydroxamic acids

    Indian Academy of Sciences (India)

    Sneha Karmarkar; P V Khadikar; Vijay K Agrawal; Keshav C Mathur; Manorama Mandloi; Shobha Joshi

    2000-02-01

    Proton-ligand formation constants of salicylhydroxamic acids (SHA) and their nuclear substituted derivatives have been estimated topologically using the normalized Wiener index, referred to as mean square Wiener index (Wms). Regression analysis of the data indicates that Wms can be used successfully for estimating and monitoring proton-ligand formation constants.

  6. Dimercaptosuccinic acid: A multifunctional cost effective agent for imaging and therapy

    International Nuclear Information System (INIS)

    Dimercaptosuccinic acid (DMSA) is an analog of dimercaprol used as metal chelating moiety in variety of conditions. In nuclear medicine itself two types of Tc-99m DMSA complexes are used, trivalent and pentavalent forms. In this review, we have discussed the mechanism of uptake of both complexes as well as diagnostic and therapeutic application in a clinical scenario

  7. Sugar beet pulp and poly(lactic acid) composites using methylene diphenyl diisocyanate as coupling agent

    Science.gov (United States)

    Composites from sugar beet pulp (SBP) and poly(lactic acid) (PLA) were extruded in the presence of polymeric methylene diphenyl diisocyanate (pMDI). SBP particles were evenly distributed within the PLA matrix phase as revealed by confocal fluorescence microscopic analysis. The resultant composites w...

  8. Synthesis, isolation and identification of glucuronides and mercapturic acids of a novel antiparasitic agent, licochalcone A

    DEFF Research Database (Denmark)

    Nadelmann, L.; Tjornelund, J.; Hansen, S. H.;

    1997-01-01

    1. Four glucuronic acid conjugates of licochalcone A (Lica), and their metabolites, have been synthesized using rabbit and pig liver microsomes and purified by preparative hplc. 2. The glucuronides were identified as E-Lica 4'-O-beta-glucuronide, E and Z-Lica 4-O-beta-glucuronide and a mono-glucu...

  9. Synthesis of New Functionalized Citric Acid-based Dendrimers as Nanocarrier Agents for Drug Delivery

    Directory of Open Access Journals (Sweden)

    Sanaz Motamedi

    2011-06-01

    Full Text Available Introduction: Citric acid-polyethylene glycol-citric acid (CPEGC triblock dendrimers can serve as potential delivery systems. Methods: In this investigation, CPEGC triblock dendrimers were synthesized and then imidazole groups were conjugated onto the surface of the G1, G2 and G3 of the obtained dendrimers. In order to study the type of the interactions between the functionalized dendrimers and a drug molecule, Naproxen which contains acidic groups, was examined as a hydrophobic drug in which the interactions would be of the electrostatic kind between its acidic groups and the lone pair electrons of nitrogen atom in imidazole groups. The quantity of the trapped drug and also the amount of its release were measured with UV spectrometric method in pH 1, 7.4 and 10. The average diameter of the nanocarriers was measured by Dynamic Light Scattering (DLS technique Results: The size range of particles was determined to be 16-50 nm for different generations. The rate of the release increased in pH=10 in all generations due to the increase in Naproxen solubility and the hydrolysis of the esteric bonds in the mentioned pH. The results showed that the amount of the trapped drug increased with the increase in the generation of the dendrimer and pH. Conclusion: Based on our findings, we suggest CPEGC triblock dendrimers possess great potential to be used as drug/gene delivery system.

  10. Evaluation of the metabolism in rat hearts of two new radioiodinated 3-methyl-branched fatty acid myocardial imaging agents

    International Nuclear Information System (INIS)

    The biological fate of two new radioiodinated 3-methyl-branched fatty acids has been evaluated in rat hearts following intravenous administration. Methyl-branching was introduced in [15-(p-iodophenyl)-3-R,S-methylpentadecanoic acid (BMIPP) and 15-(p-iodophenyl)-3,3-dimethylpentadecanoic acid (DMIPP) to inhibit β-oxidation. The goals of these studies were to correlate the effects of methyl-branching on the incorporation of these agents into the various fatty acid pools and subcellular distribution profiles, and to relate these data to the myocardial retention properties. The properties of BMIPP and DMIPP were compared with the 15-(p-iodophenyl)pentadecanoic acid straight-chain analogue (IPP). Differences in the heart retention of the analogues after intravenous administration in rats correlated with differences observed in subcellular distribution patterns. The dimethyl DMIPP analogue showed the longest retention and the highest association with the mitochondrial and microsomal fractions (34%, 38%) 30 min after injection. These data are in contrast to the rapid clearance of the straight-chain IPP analogue which showed much lower relative association with the mitochondria and microsomes (18%, 15%). The distribution patterns of each analogue in the various lipid pools appeared consistent with the expected capacity of the analogues to be metabolized by β-oxidation. In contrast to the rapid oxidation of the straight-chain IPP analogue, the 3-monomethyl BMIPP analogue appeared to undergo slower oxidation and clearance, whereas the dimethyl-branched DMIPP analogue was apparatently not catabolized by the myocardium. All three analogues showed some incorporation into triglycerides. The metabolism patterns of the branched analogues reported here may provide useful information in the description of the mechanisms by which BMIPP and DMIPP are retained in rat myocardium. (orig.)

  11. Citrus Flavanones Affect Hepatic Fatty Acid Oxidation in Rats by Acting as Prooxidant Agents

    OpenAIRE

    Rodrigo Polimeni Constantin; Gilson Soares do Nascimento; Renato Polimeni Constantin; Clairce Luzia Salgueiro; Adelar Bracht; Emy Luiza Ishii-Iwamoto; Nair Seiko Yamamoto; Jorgete Constantin

    2013-01-01

    Citrus flavonoids have a wide range of biological activities and positive health effects on mammalian cells because of their antioxidant properties. However, they also act as prooxidants and thus may interfere with metabolic pathways. The purpose of this work was to evaluate the effects of three citrus flavanones, hesperidin, hesperetin, and naringenin, on several parameters linked to fatty acid oxidation in mitochondria, peroxisomes, and perfused livers of rats. When exogenous octanoate was ...

  12. Nucleic Acid Aptamers as Potential Therapeutic and Diagnostic Agents for Lymphoma

    OpenAIRE

    Shum, Ka-To; Zhou, Jiehua; John J. Rossi

    2013-01-01

    Lymphomas are cancers that arise from white blood cells and usually present as solid tumors. Treatment of lymphoma often involves chemotherapy, and can also include radiotherapy and/or bone marrow transplantation. There is an un-questioned need for more effective therapies and diagnostic tool for lymphoma. Aptamers are single stranded DNA or RNA oligonucleotides whose three-dimensional structures are dictated by their sequences. The immense diversity in function and structure of nucleic acids...

  13. Conversion of glucose to fatty acids and methane: roles of two mycoplasmal agents.

    OpenAIRE

    Rose, C S; Pirt, S J

    1981-01-01

    Two species of obligately anaerobic mycoplasmas were the major components of a methanogenic glucose-limited enrichment culture. In pure culture, one of these organisms, tentatively named Anaeroplasma sp. strain London, was shown to be responsible for the fermentation of glucose to fatty acids, hydrogen, and carbon dioxide; the other mycoplasma was shown to produce methane from hydrogen and carbon dioxide and was named Methanoplasma elizabethii. This same methanogenic mycoplasma contained a lo...

  14. Development of antiproliferative nanohybrid compound with controlled release property using ellagic acid as the active agent

    OpenAIRE

    Hussein MZ; Al Ali SH; Zainal Z; Hakim MN

    2011-01-01

    Mohd Zobir Hussein1,2, Samer Hasan Al Ali2, Zulkarnain Zainal2, Muhammad Nazrul Hakim31Advanced Materials and Nanotechnology Laboratory, Institute of Advanced Technology (ITMA), 2Department of Chemistry, Faculty of Science, 3Department of Biomedical Science, Faculty of Medicine and Health Science, Universiti Putra Malaysia, Selangor, MalaysiaAbstract: An ellagic acid (EA)–zinc layered hydroxide (ZLH) nanohybrid (EAN) was synthesized under a nonaqueous environment using EA and zinc o...

  15. Bioprospecting the Curculigoside-Cinnamic Acid-Rich Fraction from Molineria latifolia Rhizome as a Potential Antioxidant Therapeutic Agent.

    Science.gov (United States)

    Ooi, Der Jiun; Chan, Kim Wei; Sarega, Nadarajan; Alitheen, Noorjahan Banu; Ithnin, Hairuszah; Ismail, Maznah

    2016-01-01

    Increasing evidence from both experimental and clinical studies depicts the involvement of oxidative stress in the pathogenesis of various diseases. Specifically, disruption of homeostatic redox balance in accumulated body fat mass leads to obesity-associated metabolic syndrome. Strategies for the restoration of redox balance, potentially by exploring potent plant bioactives, have thus become the focus of therapeutic intervention. The present study aimed to bioprospect the potential use of the curculigoside-cinnamic acid-rich fraction from Molineria latifolia rhizome as an antioxidant therapeutic agent. The ethyl acetate fraction (EAF) isolated from M. latifolia rhizome methanolic extract (RME) contained the highest amount of phenolic compounds, particularly curculigoside and cinnamic acid. EAF demonstrated glycation inhibitory activities in both glucose- and fructose-mediated glycation models. In addition, in vitro chemical-based and cellular-based antioxidant assays showed that EAF exhibited high antioxidant activities and a protective effect against oxidative damage in 3T3-L1 preadipocytes. Although the efficacies of individual phenolics differed depending on the structure and concentration, a correlational study revealed strong correlations between total phenolic contents and antioxidant capacities. The results concluded that enriched phenolic contents in EAF (curculigoside-cinnamic acid-rich fraction) contributed to the overall better reactivity. Our data suggest that this bioactive-rich fraction warrants therapeutic potential against oxidative stress-related disorders. PMID:27322226

  16. Potential cerebral perfusion agents: synthesis and evaluation of a radioiodinated vinylalkylbarbituric acid analogue

    International Nuclear Information System (INIS)

    A new iodinated barbiturate has been prepared. Treatment of 5-chloropentyne and propargyl bromide with diethyl 2-ethyl-2-sodiomalonate (DESM) provided diethyl 2-ethyl-2-(1-pentyn-5-yl)malonate (3) and diethyl 2-ethyl-2-propargylmalonate (4), respectively. Similar condensation of DESM with (E)-(5-iodo-1-penten-1-yl)boronic acid (9) or the reaction of catecholborane with 3 provided diethyl (E)-2-ethyl-2-(1-borono-1-penten-5-yl)malonate (8). The direct sodium iodide-chloramine-T iodination of 8 or the treatment of (E)-1,5-diiodo-1-pentene (10) with DESM provided diethyl (E)-2-ethyl-2-(1-iodo-1-penten-5-yl)malonate (11). The condensation of functionalized malonates 3, 4, and 11 with urea in the presence of a base provided the corresponding barbiturates, 5-ethyl-5-(1-pentyn-5-yl)-(5), 5-ethyl-5-propargyl- (6), and (E)-5-ethyl-5-(1-iodo-1-penten-5-yl)barbituric acid (12), respectively. (E)-6-(Ethoxycarbonyl)-1-iodo-1-octene-6-carboxylic acid (13) was isolated as the hydrolytic byproduct of 11. Compound 13 decarboxylated under vacuum to provide ethyl (E)-1-iodo-1-octene-6-carboxylate (14). The 125I-labeled congeners of 12 and 13 were synthesized in the same manner and evaluated in rats. The barbiturate 12 exhibited significant brain uptake (approximately 1% dose after 5 min), demonstrating that iodinated barbiturates freely cross the intact blood-brain barrier

  17. Potential cerebral perfusion agents: synthesis and evaluation of a radioiodinated vinylalkylbarbituric acid analogue

    Energy Technology Data Exchange (ETDEWEB)

    Srivastava, P.C.; Callahan, A.P.; Cunningham, E.B.; Knapp, F.F. Jr.

    1983-05-01

    A new iodinated barbiturate has been prepared. Treatment of 5-chloropentyne and propargyl bromide with diethyl 2-ethyl-2-sodiomalonate (DESM) provided diethyl 2-ethyl-2-(1-pentyn-5-yl)malonate (3) and diethyl 2-ethyl-2-propargylmalonate (4), respectively. Similar condensation of DESM with (E)-(5-iodo-1-penten-1-yl)boronic acid (9) or the reaction of catecholborane with 3 provided diethyl (E)-2-ethyl-2-(1-borono-1-penten-5-yl)malonate (8). The direct sodium iodide-chloramine-T iodination of 8 or the treatment of (E)-1,5-diiodo-1-pentene (10) with DESM provided diethyl (E)-2-ethyl-2-(1-iodo-1-penten-5-yl)malonate (11). The condensation of functionalized malonates 3, 4, and 11 with urea in the presence of a base provided the corresponding barbiturates, 5-ethyl-5-(1-pentyn-5-yl)-(5), 5-ethyl-5-propargyl- (6), and (E)-5-ethyl-5-(1-iodo-1-penten-5-yl)barbituric acid (12), respectively. (E)-6-(Ethoxycarbonyl)-1-iodo-1-octene-6-carboxylic acid (13) was isolated as the hydrolytic byproduct of 11. Compound 13 decarboxylated under vacuum to provide ethyl (E)-1-iodo-1-octene-6-carboxylate (14). The /sup 125/I-labeled congeners of 12 and 13 were synthesized in the same manner and evaluated in rats. The barbiturate 12 exhibited significant brain uptake (approximately 1% dose after 5 min), demonstrating that iodinated barbiturates freely cross the intact blood-brain barrier.

  18. Intravenous Immunoglobulin and Mycophenolate Mofetil for Long-Standing Sensory Neuronopathy in Sjögren's Syndrome

    Directory of Open Access Journals (Sweden)

    Maria Giovanna Danieli

    2012-01-01

    Full Text Available Sensory neuronopathy is described in association with the Sjögren's syndrome (SS. We studied a 55-year-old woman with a 4-year history of progressive asymmetric numbness, distal tingling, and burning sensation in upper and lower limbs. In a few months, she developed ataxia with increased hypoanaesthesia. Electrodiagnostic tests revealed undetectable distal and proximal sensory nerve action potential in upper and lower limbs. Cervical spine magnetic resonance showed a signal hyperintensity of posterior columns. Previous treatment with high-dose glucocorticoids and azathioprine was ineffective. A combined treatment with intravenous immunoglobulin and mycophenolate mofetil was followed by a progressive and persistent improvement. This case documented the efficacy and the safety of the coadministration of intravenous immunoglobulin and mycophenolate mofetil in sensory neuronopathy associated with SS refractory to conventional immunosuppressive therapy.

  19. Intravenous Immunoglobulin and Mycophenolate Mofetil for Long-Standing Sensory Neuronopathy in Sjögren's Syndrome.

    Science.gov (United States)

    Danieli, Maria Giovanna; Pettinari, Lucia; Morariu, Ramona; Monteforte, Fernando; Logullo, Francesco

    2012-01-01

    Sensory neuronopathy is described in association with the Sjögren's syndrome (SS). We studied a 55-year-old woman with a 4-year history of progressive asymmetric numbness, distal tingling, and burning sensation in upper and lower limbs. In a few months, she developed ataxia with increased hypoanaesthesia. Electrodiagnostic tests revealed undetectable distal and proximal sensory nerve action potential in upper and lower limbs. Cervical spine magnetic resonance showed a signal hyperintensity of posterior columns. Previous treatment with high-dose glucocorticoids and azathioprine was ineffective. A combined treatment with intravenous immunoglobulin and mycophenolate mofetil was followed by a progressive and persistent improvement. This case documented the efficacy and the safety of the coadministration of intravenous immunoglobulin and mycophenolate mofetil in sensory neuronopathy associated with SS refractory to conventional immunosuppressive therapy. PMID:25383230

  20. Application of lactobionic acid and nonionic surfactants as solubilizing agents for parenteral formulation of clarithromycin

    OpenAIRE

    Mohammad-Hosein Zarrintan; Hadi Valizadeh; Saeed Ghanbarzadeh; Parvin Zakeri-Milani; Niaz Mousavian-Fathi

    2012-01-01

    Purpose: The purpose of this paper is to enhance the solubility of clarithromycin (CLR) using nonionic surfactants and some type of acids for preparation of the new formulations. Methods: Myrj 52 and chremophor (2.5 and 5% w/v) were used in two concentrations. To investigate solubility, the formulations were shaken for 48 hours at room temperature. For stability test, lyophilized samples were maintained in refrigerator at 4° C, and in oven at 40° C. Drug analysis was performed by reverse phas...

  1. Synthesis and Conformation of Novel 4'-Fluorinated 5'-Deoxythreosyl Phosphonic Acid Nucleosides as Antiviral Agents

    International Nuclear Information System (INIS)

    Efficient synthetic route to novel 4'-fluorinated 5'-deoxythreosyl phosphonic acid nucleosides was described from glyceraldehyde using Horner-Emmons reaction in the presence of triethyl α-fluorophosphonoacetate. Glycosylation reaction of nucleosidic bases with glycosly donor 14 gave the nucleosides which were further phosphonated and hydrolyzed to reach desired nucleoside analogues. Synthesized nucleoside analogues 18, 21, 25 and 28 were tested for anti-HIV activity as well as cytotoxicity. Adenine derivatives 18 and 21 showed significant anti-HIV activity up to 100 μM

  2. Can propolis and caffeic acid phenethyl ester (CAPE be promising agents against cyclophosphamide toxicity?

    Directory of Open Access Journals (Sweden)

    Sumeyya Akyol

    2016-03-01

    Full Text Available Propolis is a mixture having hundreds of polyphenols including caffeic acid phenethyl ester (CAPE. They have been using in several medical conditions/diseases in both in vitro and in vivo experimental setup. Cyclophosphamide has been used to treat a broad of malignancies including Hodgkin's and non-Hodgking's lymphoma, Burkitt's lymphoma, chronic lymphocytic leukemia, Ewing's sarcoma, breast cancer, testicular cancer, etc. It may cause several side effects after treatment. In this mini review, the protective effects of propolis and CAPE were compared each other in terms of effectiveness against cyclophosphamide-induced injuries. [J Intercult Ethnopharmacol 2016; 5(1.000: 105-107

  3. Engineering Human T Cells for Resistance to Methotrexate and Mycophenolate Mofetil as an In Vivo Cell Selection Strategy

    OpenAIRE

    Mahesh Jonnalagadda; Brown, Christine E; Wen-Chung Chang; Ostberg, Julie R.; Forman, Stephen J.; Jensen, Michael C.

    2013-01-01

    Gene transfer and drug selection systems that enforce ongoing transgene expression in vitro and in vivo which are compatible with human pharmaceutical drugs are currently underdeveloped. Here, we report on the utility of incorporating human enzyme muteins that confer resistance to the lymphotoxic/immunosuppressive drugs methotrexate (MTX) and mycophenolate mofetil (MMF) in a multicistronic lentiviral vector for in vivo T lymphocyte selection. We found that co-expression of human dihydrofolate...

  4. I-123-labelled heptadecanoic acid as myocardial imaging agent: comparison with thallium-201 and first-pass nuclear ventriculography

    International Nuclear Information System (INIS)

    Results of the use of 123I-iodoheptadecanoic acid (HA) as a myocardial imaging agent in eight patients and six normals are presented. It was shown that 123I-HA gave comparable results to the widely used radiopharmaceutical 201Tl. However the advantages of using 123I-HA are that the 159 KeV energy is better suited to the conventional gamma camera, it gives a lower radiation dose to the patient and has a lower cost per study. 123I-HA also has an important advantage in its potential for studying regional myocardial metabolic activity; in one patient, a defect due to ischaemia was seen at rest with 123I-HA but required stress to make it evident with 201Tl imaging. (U.K.)

  5. Novel 3,4-seco bile acid diamides as selective anticancer proliferation and migration agents.

    Science.gov (United States)

    Mao, Shi-Wei; Chen, Huang; Yu, Li-Fang; Lv, Fang; Xing, Ya-Jing; Liu, Ting; Xie, Jia; Tang, Jie; Yi, Zhengfang; Yang, Fan

    2016-10-21

    A series of new seco-A ring bile acid diamides were synthesized, and their antiproliferative activities against PC3M (prostate), HT29 (colon) and ES-2 (ovarian) cancer cell lines were investigated using SRB assays. Most synthesized compounds presented improved antiproliferative activities compared to the parent bile acids (IC50 > 80 μM), especially the piperazine conjugated compound 27 with IC50 values of 1.07, 4.58 and 3.86 μM against PC3M, HT29 and ES-2 cancer cell lines, respectively. In addition, all the tested compounds showed less cytotoxic activity on a noncancerous cell line (HAF), and the most active compound 27 exhibited the highest selectivity (Selectivity Index, SI(PC3M) = 26.3). Furthermore, 27 could also enhance G1 arrest in PC3M cell, revealed by cell cycle analysis, and increase anti-migration activity on PC3M cells, confirmed by transwell migration assay. PMID:27448915

  6. Application of lactobionic acid and nonionic surfactants as solubilizing agents for parenteral formulation of clarithromycin

    Directory of Open Access Journals (Sweden)

    Mohammad-Hosein Zarrintan

    2012-06-01

    Full Text Available Purpose: The purpose of this paper is to enhance the solubility of clarithromycin (CLR using nonionic surfactants and some type of acids for preparation of the new formulations. Methods: Myrj 52 and chremophor (2.5 and 5% w/v were used in two concentrations. To investigate solubility, the formulations were shaken for 48 hours at room temperature. For stability test, lyophilized samples were maintained in refrigerator at 4° C, and in oven at 40° C. Drug analysis was performed by reverse phase high performance liquid chromatography (HPLC with ultraviolet detection. Results: Solubility tests indicated that lactobionic acid was the most effective to increase clarithromycin solubility and chremophor showed higher enhancing effect than myrj 52 on CLR solubility. The stability tests results also confirmed that shelf-lives of all formulations have been the equivalent to 24 months. Conclusion: On the whole, formulations described in this article may be very suitable for industrial-scale manufacturing and clinical application.

  7. NIR and visible investigation of some potential SERS-active substrates for studying antitumour agent all- trans retinoic acid

    Science.gov (United States)

    Beljebbar, A.; Sockalingum, G. D.; Morjani, H.; Angiboust, J. F.; Manfait, M.

    1997-01-01

    Red and near-infrared excited Fourier transform surface-enhanced Raman spectra of an anticancer agent, all- trans retinoic acid (ATRA), adsorbed on gold island films are reported. Best results have been obtained with plates 80 Å and 40 Å thick respectively in the red and near-infrared and at concentrations of 10 -5 and 5 × 10 -6 M with a spinning system. The use of near-infrared laser excitation with low photon energy, allows us to overcome the problems of isomerisation when the sample is exposed for a long time to the laser radiation. Comparison between the Raman and SERS spectra in the visible shows that the adsorption on the surface does not perturb the structure of ATRA and confirms the long range enhancement of the island films with this type of molecule. Spectral data show that while gold island films and colloids are appropriate substrates for use with red excitation, silver and gold colloids as well as gold island films exhibit satisfactory enhancement levels in the near-infrared. This study will in the future allow us to choose the appropriate system that will serve to investigate the interaction of ATRA with its target in vitro and the effect of this differentiating agent in human leukaemia cell lines such as K562 and HL60.

  8. Mycophenolate mofetil combined with steroids: New experiences in the treatment of idiopathic retroperitoneal fibrosis

    Directory of Open Access Journals (Sweden)

    Obrenčević Katarina

    2007-01-01

    Full Text Available Background/Aim. Idiopathic retroperitoneal fibrosis (IRF is an uncommon disease characterized by a retroperitoneal fibrotic tissue that often involve the ureters, leading to the obstructive nephropathy and variable impairment of renal function. Findings strongly suggest an autoimmune etiology. Surgery, medical treatment with immunosuppressive drugs, or a combination of both are proposed. The optimal treatment has not been established yet. The aim of this study was to present our experience with combined immunosuppressive therapy of IRF, steroids (S and mycophenolate mofetil (MMF. Methods. We prospectively followed four patients with IRF from January 2004 to December 2006. Three patients had an active disease with bilateral hydronephrosis. In the two of them acute renal failure was presented, and ureteral catheters were inserted in one in order to manage ureteral obstruction. One patient has came to our unit with a relapse of IRF and incipient chronic renal failure after the prior therapy with ureterolysis and immunosuppressive drugs (azathioprine and tamoxifen. All patients received steroids and MMF. Two patients were treated with intravenous methylprednisolone pulses (250 mg each, for three consecutive days, followed by oral prednisone 0.5 mg/kg/day. The other two patients received oral prednisone at the same dose. Prednisone was gradually tappered to a maintenance dose of 10 mg/kg/day. Simultaneously, all patients received MMF, initially 1 g/day with the increase to 2 g/day. Results. After four weeks of the therapy all symptoms disappeared, as well as a hydronephrosis with a decrease of erythrocyte sedimentation rate and Creactive protein (CRP to normal level in all patients. Three patients remain in remission untill the end of the follow up. One patient had a relapse because of stopping taking the therapy after six months. He was treated by oral prednisone 0.5 mg/kg/day, which was gradually decreased. After twelve weeks hydronephrosis

  9. Synthesis of Water-Dispersible Maghemite Nanocrystals using 6-Aminohexanoic Acid as a Capping Agent

    International Nuclear Information System (INIS)

    This paper describes a simple route to synthesis of water-dispersible monodisperse maghemite (γ-Fe2O3) nanocrystals using 6-aminohexanoic acid (AHA) as a stabilizer. The water-dispersible γ-Fe2O3 nanocrystals with an average size of 5 nm were obtained simply by addition of Fe(CO)5 into an octyl ether solution containing AHA at 195 .deg. C under argon condition. As-prepared AHA coated γ-Fe2O3 nanocrystals exhibited highly crystallinity and magnetic property while keeping a good dispersity in an aqueous phase. We also obtained water-dispersible AHA coated γ-Fe2O3 nanocrystals using ligand-exchange method, demonstrating that AHA can be a good candidate for preparing water-dispersible uniform metal oxide nanocrystals

  10. Estimation of very low concentrations of Ruthenium by spectrophotometric method using barbituric acid as complexing agent

    International Nuclear Information System (INIS)

    Spectrophotometric method employing numerous chromogenic reagents like thiourea, 1,10-phenanthroline, thiocyanate and tropolone is reported in the literature for the estimation of very low concentrations of Ru. A sensitive spectrophotometric method has been developed for the determination of ruthenium in the concentration range 1.5 to 6.5 ppm in the present work. This method is based on the reaction of ruthenium with barbituric acid to produce ruthenium(ll)tris-violurate, (Ru(H2Va)3)-1 complex which gives a stable deep-red coloured solution. The maximum absorption of the complex is at 491 nm due to the inverted t2g → Π(L-L ligand) electron - transfer transition. The molar absorptivity of the coloured species is 9,851 dm3 mol-1 cm-1

  11. Influence of pH, bleaching agents, and acid etching on surface wear of bovine enamel

    Directory of Open Access Journals (Sweden)

    Ana Flávia Soares

    2016-02-01

    Full Text Available ABSTRACT Development of new materials for tooth bleaching justifies the need for studies to evaluate the changes in the enamel surface caused by different bleaching protocols. Objective The aim of this study was to evaluate the bovine dental enamel wear in function of different bleaching gel protocols, acid etching and pH variation. Material and Methods Sixty fragments of bovine teeth were cut, obtaining a control and test areas. In the test area, one half received etching followed by a bleaching gel application, and the other half, only the bleaching gel. The fragments were randomly divided into six groups (n=10, each one received one bleaching session with five hydrogen peroxide gel applications of 8 min, activated with hybrid light, diode laser/blue LED (HL or diode laser/violet LED (VHL (experimental: Control (C; 35% Total Blanc Office (TBO35HL; 35% Lase Peroxide Sensy (LPS35HL; 25% Lase Peroxide Sensy II (LPS25HL; 15% Lase Peroxide Lite (LPL15HL; and 10% hydrogen peroxide (experimental (EXP10VHL. pH values were determined by a pHmeter at the initial and final time periods. Specimens were stored, subjected to simulated brushing cycles, and the superficial wear was determined (μm. ANOVA and Tukey´s tests were applied (α=0.05. Results The pH showed a slight decrease, except for Group LPL15HL. Group LPS25HL showed the highest degree of wear, with and without etching. Conclusion There was a decrease from the initial to the final pH. Different bleaching gels were able to increase the surface wear values after simulated brushing. Acid etching before bleaching increased surface wear values in all groups.

  12. Influence of pH, bleaching agents, and acid etching on surface wear of bovine enamel

    Science.gov (United States)

    Soares, Ana Flávia; Bombonatti, Juliana Fraga Soares; Alencar, Marina Studart; Consolmagno, Elaine Cristina; Honório, Heitor Marques; Mondelli, Rafael Francisco Lia

    2016-01-01

    ABSTRACT Development of new materials for tooth bleaching justifies the need for studies to evaluate the changes in the enamel surface caused by different bleaching protocols. Objective The aim of this study was to evaluate the bovine dental enamel wear in function of different bleaching gel protocols, acid etching and pH variation. Material and Methods Sixty fragments of bovine teeth were cut, obtaining a control and test areas. In the test area, one half received etching followed by a bleaching gel application, and the other half, only the bleaching gel. The fragments were randomly divided into six groups (n=10), each one received one bleaching session with five hydrogen peroxide gel applications of 8 min, activated with hybrid light, diode laser/blue LED (HL) or diode laser/violet LED (VHL) (experimental): Control (C); 35% Total Blanc Office (TBO35HL); 35% Lase Peroxide Sensy (LPS35HL); 25% Lase Peroxide Sensy II (LPS25HL); 15% Lase Peroxide Lite (LPL15HL); and 10% hydrogen peroxide (experimental) (EXP10VHL). pH values were determined by a pHmeter at the initial and final time periods. Specimens were stored, subjected to simulated brushing cycles, and the superficial wear was determined (μm). ANOVA and Tukey´s tests were applied (α=0.05). Results The pH showed a slight decrease, except for Group LPL15HL. Group LPS25HL showed the highest degree of wear, with and without etching. Conclusion There was a decrease from the initial to the final pH. Different bleaching gels were able to increase the surface wear values after simulated brushing. Acid etching before bleaching increased surface wear values in all groups. PMID:27008254

  13. Influence of pH, bleaching agents, and acid etching on surface wear of bovine enamel.

    Science.gov (United States)

    Soares, Ana Flávia; Bombonatti, Juliana Fraga Soares; Alencar, Marina Studart; Consolmagno, Elaine Cristina; Honório, Heitor Marques; Mondelli, Rafael Francisco Lia

    2016-02-01

    Development of new materials for tooth bleaching justifies the need for studies to evaluate the changes in the enamel surface caused by different bleaching protocols. Objective The aim of this study was to evaluate the bovine dental enamel wear in function of different bleaching gel protocols, acid etching and pH variation. Material and Methods Sixty fragments of bovine teeth were cut, obtaining a control and test areas. In the test area, one half received etching followed by a bleaching gel application, and the other half, only the bleaching gel. The fragments were randomly divided into six groups (n=10), each one received one bleaching session with five hydrogen peroxide gel applications of 8 min, activated with hybrid light, diode laser/blue LED (HL) or diode laser/violet LED (VHL) (experimental): Control (C); 35% Total Blanc Office (TBO35HL); 35% Lase Peroxide Sensy (LPS35HL); 25% Lase Peroxide Sensy II (LPS25HL); 15% Lase Peroxide Lite (LPL15HL); and 10% hydrogen peroxide (experimental) (EXP10VHL). pH values were determined by a pHmeter at the initial and final time periods. Specimens were stored, subjected to simulated brushing cycles, and the superficial wear was determined (μm). ANOVA and Tukey´s tests were applied (α=0.05). Results The pH showed a slight decrease, except for Group LPL15HL. Group LPS25HL showed the highest degree of wear, with and without etching. Conclusion There was a decrease from the initial to the final pH. Different bleaching gels were able to increase the surface wear values after simulated brushing. Acid etching before bleaching increased surface wear values in all groups. PMID:27008254

  14. Development of antiproliferative nanohybrid compound with controlled release property using ellagic acid as the active agent

    Directory of Open Access Journals (Sweden)

    Hussein MZ

    2011-07-01

    Full Text Available Mohd Zobir Hussein1,2, Samer Hasan Al Ali2, Zulkarnain Zainal2, Muhammad Nazrul Hakim31Advanced Materials and Nanotechnology Laboratory, Institute of Advanced Technology (ITMA, 2Department of Chemistry, Faculty of Science, 3Department of Biomedical Science, Faculty of Medicine and Health Science, Universiti Putra Malaysia, Selangor, MalaysiaAbstract: An ellagic acid (EA–zinc layered hydroxide (ZLH nanohybrid (EAN was synthesized under a nonaqueous environment using EA and zinc oxide (ZnO as the precursors. Powder X-ray diffraction showed that the basal spacing of the nanohybrid was 10.4 Å, resulting in the spatial orientation of EA molecules between the interlayers of 22.5° from z-axis with two negative charges at 8,8′ position of the molecules pointed toward the ZLH interlayers. FTIR study showed that the intercalated EA spectral feature is generally similar to that of EA, but with bands slightly shifted. This indicates that some chemical bonding of EA presence between the nanohybrid interlayers was slightly changed, due to the formation of host–guest interaction. The nanohybrid is of mesopores type with 58.8% drug loading and enhanced thermal stability. The release of the drug active, EA from the nanohybrid was found to be sustained and therefore has good potential to be used as a drug controlled-release formulation. In vitro bioassay study showed that the EAN has a mild effect on the hepatocytes cells, similar to its counterpart, free EA.Keywords: ellagic acid, nonaqueous solution, ZnO, zinc-layered hydroxide, viability test

  15. Antiretroviral agents and acid-base balance at delivery of the neonate

    Directory of Open Access Journals (Sweden)

    P. El-Beitune

    2007-07-01

    Full Text Available Limited evidence is available regarding antiretroviral (ARV safety for uninfected infants exposed to these drugs in utero. Our objective was to determine if ARV administered to pregnant women is associated with decreasing umbilical arterial pH and base excess in uninfected infants. A prospective study was conducted on 57 neonates divided into three groups: ZDV group, born to mothers taking zidovudine (N = 20, triple therapy (TT group, born to mothers taking zidovudine + lamivudine + nelfinavir (N = 25, and control group (N = 12, born to uninfected mothers. Umbilical cord blood was used to determine umbilical artery gases. A test was performed to calculate the sample by comparing means by the unpaired one-tailed t-test, with a = 0.05 and ß = 20%, indicating the need for a sample of 18 newborn infants for the study groups to detect differences higher than 20%. The control and ARV groups were similar in gestational age, birth weight, and Apgar scores. Values of pH, pCO2, bicarbonate, and base excess in cord arterial blood obtained at delivery from the newborns exposed to TT were 7.23, 43.2 mmHg, 19.5 mEq/L, and -8.5 nmol/L, respectively, with no significant difference compared to the control and ZDV groups. We conclude that intrauterine exposure to ARV is not associated with a pathological decrease in umbilical arterial pH or base excess. While our data are reassuring, follow-up is still limited and needs to be continued into adulthood because of the possible potential for adverse effects of triple antiretroviral agents.

  16. Benzyl and Methyl Fatty Hydroxamic Acids Based on Palm Kernel Oil as Chelating Agent for Liquid-Liquid Iron(III) Extraction

    OpenAIRE

    Jamileh Amin; Roshanak Rafiee-Moghaddam; Behnam Mahdavi; Mazyar Peyda; Anuar Kassim; Nor Azah Yusof; Md Jelas Haron; Hossein Jahangirian; Yadollah Abdollahi; Sidik Silong

    2012-01-01

    Liquid-liquid iron(III) extraction was investigated using benzyl fatty hydroxamic acids (BFHAs) and methyl fatty hydroxamic acids (MFHAs) as chelating agents through the formation of iron(III) methyl fatty hydroxamate (Fe-MFHs) or iron(III) benzyl fatty hydroxamate (Fe-BFHs) in the organic phase. The results obtained under optimized conditions, showed that the chelating agents in hexane extract iron(III) at pH 1.9 were realized effectively with a high percentage of extraction (97.2% and 98.1%...

  17. Versatile methods for synthesizing organic acid salts of quaternary berberine-type alkaloids as anti-ulcerative colitis agents.

    Science.gov (United States)

    Zhang, Zhi-Hui; Li, Jing; Zhang, Hai-Jing; Deng, An-Jun; Wu, Lian-Qiu; Li, Zhi-Hong; Song, Hong-Rui; Wang, Wen-Jie; Qin, Hai-Lin

    2016-06-01

    Two versatile methods to synthesize kinds of organic acid salts of quaternary berberine-type alkaloids were investigated in order to determine which is more efficient to improve the liposolubility of the target compounds and to explore the efficacy of the target compounds as anti-ulcerative colitis (UC) agents. Overall evaluation according to the reaction results and yields of the final products indicated that the synthetic method using tertiary (±)-8-acylmethyldihydroberberine-type alkaloids as key intermediates is superior to that of using tertiary dihydroberberine-type alkaloids as intermediates. Ten target compounds were synthesized using quaternary berberine chloride and quaternary coptisine chloride as starting materials, respectively, and the anti-UC activity of some target compounds was evaluated in an in vitro x-box-binding protein 1 (XBP1) transcriptional activity assay using dual luciferase reporter detection. At 10 μM, the tested compounds were found to activate the transcription of XBP1 target at almost the same level as that of quaternary coptisine chloride. The synthesized target compounds were also found to share higher liposolubility than the inorganic acid salts of quaternary berberine-type alkaloid. PMID:27097666

  18. Oleanolic acid (OA) as an antileishmanial agent: Biological evaluation and in silico mechanistic insights.

    Science.gov (United States)

    Melo, Tahira Souza; Gattass, Cerli Rocha; Soares, Deivid Costa; Cunha, Micael Rodrigues; Ferreira, Christian; Tavares, Maurício Temotheo; Saraiva, Elvira; Parise-Filho, Roberto; Braden, Hannah; Delorenzi, Jan Carlo

    2016-06-01

    Although a worldwide health problem, leishmaniasis is considered a highly neglected disease, lacking efficient and low toxic treatment. The efforts for new drug development are based on alternatives such as new uses for well-known drugs, in silico and synthetic studies and naturally derived compounds. Oleanolic acid (OA) is a pentacyclic triterpenoid widely distributed throughout the Plantae kingdom that displays several pharmacological activities. OA showed potent leishmancidal effects in different Leishmania species, both against promastigotes (IC(50 L. braziliensis) 30.47 ± 6.35 μM; IC(50 L. amazonensis) 40.46 ± 14.21 μM; IC(50 L. infantum) 65.93 ± 15.12 μM) and amastigotes (IC(50 L. braziliensis) 68.75 ± 16.55 μM; IC(50 L. amazonensis) 38.45 ± 12.05 μM; IC(50 L. infantum) 64.08 ± 23.52 μM), with low cytotoxicity against mouse peritoneal macrophages (CC(50) 235.80 ± 36.95 μM). Moreover, in silico studies performed to evaluate OA molecular properties and to elucidate the possible mechanism of action over the Leishmania enzyme sterol 14α-demethylase (CYP51) suggested that OA interacts efficiently with CYP51 and could inhibit the ergosterol synthesis pathway. Collectively, these data indicate that OA is a good candidate as leading compound for the development of a new leishmaniasis treatment. PMID:26772973

  19. Ferulic Acid as A Potential Antioxidant Therapeutic Agent in Gamma-Irradiated Rats

    International Nuclear Information System (INIS)

    Ferulic Acid (FA) is widespread in plant foods. It possesses important biological and pharmacological properties, some of which were shown to be effective in the treatment of oxidative disorders. To investigate the therapeutic potentiality of FA on an antioxidant system of 4 Gy gamma-irradiated male rats, rats were orally administrated FA at a dosage of 200 mg/ kg body wt for 7 consecutive days. At this dose, the activities of hepatic and intestine superoxide dismutase (SOD), catalase (CAT) and glutathione peroxidase (GPx), were raised after administration of FA compared with the irradiated group (P< 0.05). Oxidized glutathione (GSSG) levels were significantly lower in the liver of rats treated with FA after irradiation, whereas reduced glutathione (GSH) was markedly higher in the same group. The liver homogenates obtained from rats that had been treated with FA had higher oxygen radical absorbance capacity (ORAC) than those obtained from irradiated rats. Peripheral leukocyte analysis revealed an increased count and restoration body wt of rats by FA treatments. These experiments show that recovery of oxidative status by FA may play an important role in the recovery from adverse effects related to gamma-rays induced oxidative damage in rats.

  20. Peracetic acid: a practical agent for sterilizing heat-labile polymeric tissue-engineering scaffolds.

    Science.gov (United States)

    Yoganarasimha, Suyog; Trahan, William R; Best, Al M; Bowlin, Gary L; Kitten, Todd O; Moon, Peter C; Madurantakam, Parthasarathy A

    2014-09-01

    Advanced biomaterials and sophisticated processing technologies aim at fabricating tissue-engineering scaffolds that can predictably interact within a biological environment at the cellular level. Sterilization of such scaffolds is at the core of patient safety and is an important regulatory issue that needs to be addressed before clinical translation. In addition, it is crucial that meticulously engineered micro- and nano- structures are preserved after sterilization. Conventional sterilization methods involving heat, steam, and radiation are not compatible with engineered polymeric systems because of scaffold degradation and loss of architecture. Using electrospun scaffolds made from polycaprolactone, a low melting polymer, and employing spores of Bacillus atrophaeus as biological indicators, we compared ethylene oxide, autoclaving and 80% ethanol to a known chemical sterilant, peracetic acid (PAA), for their ability to sterilize as well as their effects on scaffold properties. PAA diluted in 20% ethanol to 1000 ppm or above sterilized electrospun scaffolds in 15 min at room temperature while maintaining nano-architecture and mechanical properties. Scaffolds treated with PAA at 5000 ppm were rendered hydrophilic, with contact angles reduced to 0°. Therefore, PAA can provide economical, rapid, and effective sterilization of heat-sensitive polymeric electrospun scaffolds that are used in tissue engineering. PMID:24341350

  1. Synthesis and evaluation of L-glutamic acid analogs as potential anticancer agents

    Directory of Open Access Journals (Sweden)

    Viswanathan C

    2008-01-01

    Full Text Available Four N-(benzenesulfonyl-L-glutamic acid bis(p-substituted phenylhydrazides were synthesized and evaluated for anticancer activity in vitro in DU-145 and PC-3 prostate cancer and in COLO-205 colon cancer cell lines by MTT assay. The analog with the nitro group substitution exhibited potent activity (% Inhibition 84.7 and 72.0 in DU-145 and PC-3 respectively at 80 mg/ml concentration. Another series of substituted 1-(benzenesulfonyl-5-oxopyrrolidine 2-carboxamides (11a-f were synthesized and evaluated for anticancer activity in vitro in colon (COLO-205, breast (Zr-75-1 and prostate (PC-3 cancer cell lines by MTT assay using adriamycin as standard. Test compounds 11a-c showed potent activity (% Inhibition 61.2 to 79.2 at 20 mg/ml and 67.2 to 87.2 at 40 mg/ml in PC-3 cell line which is superior to the activity of Adriamycin. In comparison compounds 11d-f were less potent. In Zr-75-1 cell line 11a-e showed % inhibition ranging from 32.4 to 54.9 at 10 mg/ml concentration while in COLO-205 cell line 11a-f showed poor activity.

  2. Synthetic lethality for linking the mycophenolate mofetil mode of action with molecular disease and drug profiles.

    Science.gov (United States)

    Söllner, Johannes; Mayer, Paul; Heinzel, Andreas; Fechete, Raul; Siehs, Christian; Oberbauer, Rainer; Mayer, Bernd

    2012-10-30

    Systematic study of the effect of mycophenolate mofetil (MMF) on the molecular level in the context of other drugs and molecular disease profiles became possible due to the availability of large scale molecular profiles on both disease characterization and drug mode of action. Such analysis is of particular value in elucidating alternative drug use for addressing clinically unmet needs, and the concept of synthetic lethality provides an alternative tool for such repositioning strategies. Resting on consolidation of transcriptomics data and literature mining, a MMF molecular footprint became available including a set of 170 genes specifically affected by the drug. Analysis of this profile on a molecular pathway level reveals a set of 14 pathways as affected. Next to assignment of molecular pathways and associated diseases synergistic drug combinations are proposed by utilizing the synthetic lethal interaction network. Of particular interest is the combination of MMF with adenosine deaminase inhibitors, sulfasalazine, and other selected drugs interfering with calcium-based regulatory pathways and metabolism. Indeed analysis of drugs in clinical trials positively identifies combinations with MMF in the context of synthetic lethality and affected pathways, particularly in diseases such as multiple sclerosis, vasculitis, GVHD and lupus nephritis. Importantly, the synthetic lethal interaction of the drug mode of action is an interesting basis for rational repositioning strategies by suggesting combinations which exhibit a synergistic rather than a mere additive effect, as for example is evident for the combination of tacrolimus and MMF. Inherent is also the assessment of possible adverse effects of drug combinations. PMID:23014771

  3. Acute pancreatitis induced by mycophenolate mofetil in a kidney transplant patient

    Directory of Open Access Journals (Sweden)

    Einollahi Behzad

    2015-04-01

    Full Text Available Acute pancreatitis is a rare life-threatening complication in patients after kidney transplantation. Here we described a 56-year-old man who had received a living related kidney transplant for an end-stage renal disease. In his regular follow-up, his serum creatinine was gradually increased and he underwent an allograft biopsy, which revealed an interstitial nephritis/tubular atrophy grade II. Mycophenolate mofetil (MMF was prescribed to control chronic allograft nephropathy. He presented with complaints of severe abdominal pain, vomiting, loss of appetite and fever requiring hospital admission twelve days later. Acute pancreatitis was diagnosed on the basis of laboratory data and imaging findings during hospital admission. There was no history of alcohol consumption in our patient. Unfortunately he died one week later and autopsy findings demonstrated acute necrotizing pancreatitis. The bladder drainage of this patients was normal. Laboratory findings in this patient did not endorse infections and other possibilities regarding the etiology of acute pancreatitis in this patient. Therefore, we concluded that acute pancreatitis in near the patient was induced by drugs and basis on our evidence, MMF is the most important suspect. This study suggests that acute pancreatitis can be considered as a side effect of MMF.

  4. Oleanolic acid: a novel cardioprotective agent that blunts hyperglycemia-induced contractile dysfunction.

    Directory of Open Access Journals (Sweden)

    Rudo F Mapanga

    Full Text Available Diabetes constitutes a major health challenge. Since cardiovascular complications are common in diabetic patients this will further increase the overall burden of disease. Furthermore, stress-induced hyperglycemia in non-diabetic patients with acute myocardial infarction is associated with higher in-hospital mortality. Previous studies implicate oxidative stress, excessive flux through the hexosamine biosynthetic pathway (HBP and a dysfunctional ubiquitin-proteasome system (UPS as potential mediators of this process. Since oleanolic acid (OA; a clove extract possesses antioxidant properties, we hypothesized that it attenuates acute and chronic hyperglycemia-mediated pathophysiologic molecular events (oxidative stress, apoptosis, HBP, UPS and thereby improves contractile function in response to ischemia-reperfusion. We employed several experimental systems: 1 H9c2 cardiac myoblasts were exposed to 33 mM glucose for 48 hr vs. controls (5 mM glucose; and subsequently treated with two OA doses (20 and 50 µM for 6 and 24 hr, respectively; 2 Isolated rat hearts were perfused ex vivo with Krebs-Henseleit buffer containing 33 mM glucose vs. controls (11 mM glucose for 60 min, followed by 20 min global ischemia and 60 min reperfusion ± OA treatment; 3 In vivo coronary ligations were performed on streptozotocin treated rats ± OA administration during reperfusion; and 4 Effects of long-term OA treatment (2 weeks on heart function was assessed in streptozotocin-treated rats. Our data demonstrate that OA treatment blunted high glucose-induced oxidative stress and apoptosis in heart cells. OA therapy also resulted in cardioprotection, i.e. for ex vivo and in vivo rat hearts exposed to ischemia-reperfusion under hyperglycemic conditions. In parallel, we found decreased oxidative stress, apoptosis, HBP flux and proteasomal activity following ischemia-reperfusion. Long-term OA treatment also improved heart function in streptozotocin-diabetic rats. These

  5. Intercellular imaging by a polyarginine derived cell penetrating peptide labeled magnetic resonance contrast agent,diethylenetriamine pentaacetic acid gadolinium

    Institute of Scientific and Technical Information of China (English)

    GUO You-min; LIU Min; YANG Jun-le; GUO Xiao-juan; WANG Si-cen; DUAN Xiao-yi; WANG Peng

    2007-01-01

    Background The cellular plasma membrane represents a natural barrier to many exogenous molecules including magnetic resonance (MR) contrast agent. Cell penetrating peptide (CPP) is used to internalize proteins, peptides, and radionuclide. This study was undertaken to assess the value of a new intracellular MR contrast medium, CPP labeled diethylenetriamine pentaacetic acid gadolinium (Gd-DTPA) in molecular imaging in vitro. Methods Fluorescein-5-isothiocyanate (FITC) and Gd-DTPA respectively labeled with CPP (FITC-CPP, Gd-DTPA-CPP) were synthesized by the solid-phase method. Human hepatic cancer cell line-HepG2 was respectively stained by FITC-CPP and FITC to observe the uptake and intracellular distribution. HepG2 was respectively incubated with 100 nmol/ml Gd-DTPA-CPP for 0, 10, 30, 60 minutes, and imaged by MR for studying the relationship between the incubation time and T1WI signal. The cytotoxicity to NIH3T3 fibroblasts cells was measured by 3-(4,5-dimethylthiazol-2-yl)- 2,5-diphenyltetrazolium bromide reduction assay (MTT). Results The molecular weights of CPP labeled imaging agents, which were determined by MALDI mass spectrometry (FITC-CPP MW=2163.34, Gd-DTPA-CPP MW=2285.99), were similar to the calculated molecular weights. Confocal microscopy suggested HepG2 translocated FITC-CPP in cytoplasm and nucleus independent with the incubation temperature. MR images showed HepG2 uptaken Gd-DTPA-CPP had a higher T1 weighted imaging (T1WI) signal, and that the T1WI signal intensity was increasing in a time-dependent manner (r=0.972, P=0.001), while the signal intensity between the cells incubated by Gd-DTPA for 60 minutes and the controlled cells was not significantly different (P=0.225). By MTT, all concentrations from 50 nmol/ml to 200 nmol/ml had no significant (F=0.006, P=1.000) effect on cell viability of mouse NIH3T3 fibroblasts, compared with the control group. Conclusions The newly constructed CPP based on polyarginine can translocate cells by carrying FITC

  6. The effect of complexing agent on the extraction of Ce(III) and Nd(III) by 2-ethylhexyl phosphonic acid mono-2-ethylhexyl ester

    International Nuclear Information System (INIS)

    Liquid-liquid extraction of Ce(III) and Nd(III) has been studied using 2-ethylhexyl phosphonic acid mono-2-ethylhexyl ester (EHEHPA) in kerosene as the extractant. An improvement in separation factor between these elements has been observed in the presence of the complexing agent, glycine. (author). 6 refs., 1 tab

  7. Study of photo-oxidative reactivity of sunscreening agents based on photo-oxidation of uric acid by kinetic Monte Carlo simulation

    Energy Technology Data Exchange (ETDEWEB)

    Moradmand Jalali, Hamed; Bashiri, Hadis, E-mail: hbashiri@kashanu.ac.ir; Rasa, Hossein

    2015-05-01

    In the present study, the mechanism of free radical production by light-reflective agents in sunscreens (TiO{sub 2}, ZnO and ZrO{sub 2}) was obtained by applying kinetic Monte Carlo simulation. The values of the rate constants for each step of the suggested mechanism have been obtained by simulation. The effect of the initial concentration of mineral oxides and uric acid on the rate of uric acid photo-oxidation by irradiation of some sun care agents has been studied. The kinetic Monte Carlo simulation results agree qualitatively with the existing experimental data for the production of free radicals by sun care agents. - Highlights: • The mechanism and kinetics of uric acid photo-oxidation by irradiation of sun care agents has been obtained by simulation. • The mechanism has been used for free radical production of TiO{sub 2} (rutile and anatase), ZnO and ZrO{sub 2}. • The ratios of photo-activity of ZnO to anastase, rutile and ZrO have been obtained. • By doubling the initial concentrations of mineral oxide, the rate of reaction was doubled. • The optimum ratio of initial concentration of mineral oxides to uric acid has been obtained.

  8. Regeneration of Three-Way Automobile Catalysts using Biodegradable Metal Chelating Agent – S, S-Ethylenediamine Disuccinic Acid (S, S-EDDS)

    Science.gov (United States)

    Regeneration of the activity of three-way catalytic converters (TWCs) was tested for the first time using a biodegradable metal chelating agent (S, S. Ethylenediamine disuccinic acid (S, S-EDDS). The efficiency of this novel environmentally friendly solvent in removing various c...

  9. Study of photo-oxidative reactivity of sunscreening agents based on photo-oxidation of uric acid by kinetic Monte Carlo simulation

    International Nuclear Information System (INIS)

    In the present study, the mechanism of free radical production by light-reflective agents in sunscreens (TiO2, ZnO and ZrO2) was obtained by applying kinetic Monte Carlo simulation. The values of the rate constants for each step of the suggested mechanism have been obtained by simulation. The effect of the initial concentration of mineral oxides and uric acid on the rate of uric acid photo-oxidation by irradiation of some sun care agents has been studied. The kinetic Monte Carlo simulation results agree qualitatively with the existing experimental data for the production of free radicals by sun care agents. - Highlights: • The mechanism and kinetics of uric acid photo-oxidation by irradiation of sun care agents has been obtained by simulation. • The mechanism has been used for free radical production of TiO2 (rutile and anatase), ZnO and ZrO2. • The ratios of photo-activity of ZnO to anastase, rutile and ZrO have been obtained. • By doubling the initial concentrations of mineral oxide, the rate of reaction was doubled. • The optimum ratio of initial concentration of mineral oxides to uric acid has been obtained

  10. Some studies on the radiation-induced strand break of deoxyribonucleic acid (DNA) model systems. III. effect of repairing agents on polyribouridylic acid model systems

    International Nuclear Information System (INIS)

    The effect of repairing agents on polyuridylic acid model system has been investigated. Cysteamine and dithiothreitol (DTT) were used as radio-protectors. The effect of concentration, PH, ionic strength and counter ion on the G(ssb)-value in presence of cysteamine was studied. It was found 8% given off poly U strand break precursor radicals and the remainder 92% poly U strand break radicals were rationally repaired. A possible mechanism has been suggested. The least recorded G(ssb)-values were found at cysteamine concentration of 2 x 10-5 M in presence of 0.01 M and 0.1 M Na Cl O4. When DTT was used as a radio-protector, the rate constant K4 was half the value obtained when cystamine was used. 12% of broken strands were determined and 88% of poly U strand break radicals were repairable. When oxygen was present in the system, 42% broken poly U strands were found and only 58% of poly U strand radicals were repairable

  11. Synthesis And Characterization Of An Ion Imprinted Polymer For Cadmium Using Quinaldic Acid As Complexing Agent And Applying By Microwave

    Directory of Open Access Journals (Sweden)

    Asmawati

    2015-01-01

    Full Text Available Abstract A Cd2 Ion Imprinted Polymer Cd-IIP has been synthesized by copolymerizaton of cadmium ion quinaldic acid complexing agent 4-vynil pyridine monomer dimethyl sulfoxide solvent ethyleneglycoldimethacrylate EGDMA cross-linker and 22-azobis-isobutyronitrile AIBN initiator. Polymerization was conducted using a microwave at a temperature of 70 oC with heating times of 45 minutes. The template Cd2 was removed by leaching the template with ethanol and 4 M HCl washed by aquabidest and dried in an oven at the temperature of 60oC. The polymer particles imprinted and nonimprinted were characterized using fourir transform infrared FTIR spectroscopy scanning electron microscopy SEM and energy dispersive spectroscopy EDS. The result showed that using heating time 45 minutes at temperature 70 oC the particle morphology is viewed like as the large homogeneous. So the imprinted polymer had bands at 3483 cm-1 1726 cm-1 and 1155 cm-1 indicating the presence of OH CO and C-O respectively.

  12. Aliphatic acid-conjugated antimicrobial peptides--potential agents with anti-tumor, multidrug resistance-reversing activity and enhanced stability.

    Science.gov (United States)

    Deng, Xin; Qiu, Qianqian; Ma, Ke; Wang, Xuekun; Huang, Wenlong; Qian, Hai

    2015-07-28

    Compared with traditional therapeutics, antimicrobial peptides as novel anti-tumor agents have prominent advantages of higher specificity and circumvention of multi-drug resistance. In a previous study, we found that B1, an antimicrobial peptide derived from Cathelicidin-BF15, presented specific anti-tumor activity against several tumor cells. Since aliphatic chain-conjugated peptides have shown ameliorative activity and stability, we conjugated aliphatic acids with different lengths to the amino terminal of B1. All the conjugated peptides exhibited improved anti-tumor activity over B1. Further investigations revealed that the peptides were capable of disrupting the cell membrane, stimulating cytochrome c release into the cytosol, which results in apoptosis. The peptides also acted against multidrug resistant cells and had multidrug resistance-reversing effects. Additionally, conjugation of aliphatic acid enhanced the peptide stability in plasma. In summary, aliphatic acid-modified peptides might be promising anti-tumor agents in the future. PMID:26083110

  13. Development of novel radiogallium-labeled bone imaging agents using oligo-aspartic acid peptides as carriers.

    Directory of Open Access Journals (Sweden)

    Kazuma Ogawa

    Full Text Available (68Ga (T 1/2 = 68 min, a generator-produced nuclide has great potential as a radionuclide for clinical positron emission tomography (PET. Because poly-glutamic and poly-aspartic acids have high affinity for hydroxyapatite, to develop new bone targeting (68Ga-labeled bone imaging agents for PET, we used 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA as a chelating site and conjugated aspartic acid peptides of varying lengths. Subsequently, we compared Ga complexes, Ga-DOTA-(Aspn (n = 2, 5, 8, 11, or 14 with easy-to-handle (67Ga, with the previously described (67Ga-DOTA complex conjugated bisphosphonate, (67Ga-DOTA-Bn-SCN-HBP. After synthesizing DOTA-(Aspn by a Fmoc-based solid-phase method, complexes were formed with (67Ga, resulting in (67Ga-DOTA-(Aspn with a radiochemical purity of over 95% after HPLC purification. In hydroxyapatite binding assays, the binding rate of (67Ga-DOTA-(Aspn increased with the increase in the length of the conjugated aspartate peptide. Moreover, in biodistribution experiments, (67Ga-DOTA-(Asp8, (67Ga-DOTA-(Asp11, and (67Ga-DOTA-(Asp14 showed high accumulation in bone (10.5 ± 1.5, 15.1 ± 2.6, and 12.8 ± 1.7% ID/g, respectively but were barely observed in other tissues at 60 min after injection. Although bone accumulation of (67Ga-DOTA-(Aspn was lower than that of (67Ga-DOTA-Bn-SCN-HBP, blood clearance of (67Ga-DOTA-(Aspn was more rapid. Accordingly, the bone/blood ratios of (67Ga-DOTA-(Asp11 and (67Ga-DOTA-(Asp14 were comparable with those of (67Ga-DOTA-Bn-SCN-HBP. In conclusion, these data provide useful insights into the drug design of (68Ga-PET tracers for the diagnosis of bone disorders, such as bone metastases.

  14. Targeting T helper 17 by mycophenolate mofetil attenuates diabetic nephropathy progression.

    Science.gov (United States)

    Kim, Su-Mi; Lee, Sang-Ho; Lee, Arah; Kim, Dong-Jin; Kim, Yang-Gyun; Kim, Se-Yun; Jeong, Kyung-Hwan; Lee, Tae-Won; Ihm, Chun-Gyoo; Lim, Sung-Jig; Moon, Ju-Young

    2015-10-01

    Proinflammatory T helper 1 (Th1) and T helper 17 (Th17) cell subsets have been reported to have an immunopathogenic role in metabolic disease. We previously demonstrated that CD4(+) T cells are increased in kidneys in type 2 diabetic patients. However, the role of Th1 and Th17 cells in the development and progression of diabetic nephropathy is unclear. In this study, we examined the hypothesis that mycophenolate mofetil (MMF) attenuates diabetic kidney injury by the suppression of renal T-cell proliferation and related cytokines. Four groups of male C57/BL6 mice (8-weeks-old) were studied: (1) untreated controls, (2) MMF-treated controls (30 mg/kg of body weight per day), (3) streptozotocin (STZ)-induced diabetes, and (4) MMF-treated STZ-induced diabetes. The interferon gamma (IFN-γ) and interleukin 17 (IL-17) from renal CD4(+) T cells were analyzed in kidney mononuclear cells by flow cytometry. We found proliferating CD4(+) T cells were significantly increased in the kidney compared with the spleen. There were increases in IFN-γ(+) CD4(+) and IL-17A(+) CD4(+) T cells from the initiation of albuminuria in the kidneys of diabetic mice. We found MMF suppresses only the intrarenal IL-17A(+) CD4(+) T cells from early diabetic nephropathy and improves albuminuria, tubulointerstitial fibrosis independent of glycemic control. Our study results suggest that Th17 may play an independent role in the progression of diabetic nephropathy and modulation of IL-17 has potential as an immunologic therapeutic target. PMID:26001596

  15. Mycophenolate mofetil in the treatment of multiple sclerosis: A preliminary report

    Directory of Open Access Journals (Sweden)

    Lekha Pandit

    2014-01-01

    Full Text Available Background: Mycophenolate mofetil (MMF is an affordable and tolerable drug reported to be beneficial in the treatment of multiple sclerosis (MS. Aim: To determine efficacy of MMF as first line disease modifying drug (DMD in 40 patients with MS seen in our demyelinating disease registry. Materials and Methods: The annualized relapse rate (ARR for 1 year prior to starting MMF therapy and 1 year post treatment was calculated. Pre- and post-treatment expanded disability status scores (EDSS, age at onset of treatment, disease duration, and type of MS were recorded. Wilcoxon rank sum test was used for comparison of ARRs and EDSS before and after treatment. Results: Forty patients included 27 females and 13 males. Mean duration of MMF therapy was 24 months (range 14-33 months. Pre-treatment mean ARR of 0.95 was significantly different from post treatment mean ARR of 0.11 (P = 0.0001. Pre-treatment mean EDSS 3.80 (inter quartile range [IQR] 3.5-4.5 was significantly different from post-treatment mean EDSS 2.66 (IQR 1.5-3.0, P = 0.0001. No adverse effects were reported that required stopping of medication. Five patients discontinued treatment 6-11 months after starting therapy, two of whom relapsed subsequently. Conclusion: Our preliminary results support the use of MMF, a cheap and well-tolerated drug, as first line disease modifying drug in MS. Long-term results in a larger patient cohort is required for validating our preliminary conclusions.

  16. Feasibility of, and critical paths for mycophenolate mofetil Bayesian dose adjustment: pharmacological re-appraisal of a concentration-controlled versus fixed-dose trial in renal transplant recipients.

    Science.gov (United States)

    Prémaud, A; Rousseau, A; Le Meur, Y; Venisse, N; Loichot, C; Turcant, A; Hoizey, G; Compagnon, P; Hary, L; Debruyne, D; Saivin, S; Jacqz-Aigrain, E; Marquet, P

    2010-02-01

    The aim of this study was to analyze retrospectively and critically the different steps of the individual dose adjustment procedure employed in the concentration-controlled (CC) versus fixed-dose trial Apomygre, which showed that mycophenolate mofetil (MMF) dose adjustment using a limited sampling strategy significantly reduced the risk of treatment failures and acute rejection in renal transplants at one year posttransplantation. The number of AUCs performed during the study and circumstances of collection, time of blood sampling, Bayesian mycophenolic acid (MPA) area-under-the-curve (AUC) estimation procedures and physicians' compliance with MMF dose recommendations were retrospectively analyzed. 92% of AUCs scheduled over the study were actually performed. Sampling times were very well respected. Bayesian estimation of MPA exposure was done by the pharmacologists locally in accordance with the protocol instructions and the AUC estimates obtained were virtually all confirmed a posteriori. On the other hand, a second AUC estimated by multiple linear regression could only be provided for 84% of the profiles and showed a large overestimation with respect to Bayesian estimates for AUC values between 10 and 55mgh/L. In the CC arm, a very good physicians' compliance was observed (85%) and application of the dose recommendations led to higher values of AUCs (42.1+/-14.6mgh/L versus 36.7+/-16.3mgh/L, p=0.0035) and to more AUCs in the target range (69% versus 56%, p=0.0343) than when dose recommendations were not applied. By analyzing in detail the feasibility criteria of MMF Bayesian dose adjustment, this study highlighted the requirements for successful extrapolation of the Apomygre trial results to routine practice: (i) respect of the PK sampling time-windows; (ii) use of relevant tools for accurate drug exposure estimation and dose adjustment calculation; and (iii) good compliance of the physicians with regard to the recommended doses. PMID:19800973

  17. Determination of selenium in mice tissues to understand pharmacokinetics of diselenium propionic acid (DSePA) - a radioprotective agent

    International Nuclear Information System (INIS)

    Radiation therapy is one of the common modality for treatment of cancer which is associated with acute and chronic side effects. Recently pre-clinical and clinical studies have shown selenium analogues to be an effective radio-protective agent. One such analogue of selenium, diselenium propionic acid (DSePA), offered significant protection to normal tissue from radiotherapy induced toxicity in mice. Advanced Centre for Treatment, Research and Education in Cancer (ACTREC), Tata Memorial Centre has undertaken a systematic development of DSePA as a radioprotective agent. The plasma kinetics and biodistribution of this compound in SCID mice bearing a breast cancer xenograft has been studied. ACD supported this study by standardizing procedure for analysis of different tissue samples. About 150 samples of various tissues of mice were analyzed for Se. The following dissolution protocol was optimised. The entire tissue samples were weighed accurately in a microwave digestion vessel, to this 5 mL HNO3 and 2 mL nanopure water was added. It was subjected to an optimized digestion programme in the microwave system. Digestion of tissue samples in closed vessel microwave system ensured that there were no volatilization losses of Se, during the process. Further, nitric acid treatment ensured that Se present in the sample is converted to Se (IV). The completely dissolved sample solutions were transferred to 10 mL volumetric flask and made upto volume. Se in the solutions was determined using optimized graphite furnace program. To minimize volatilization losses during atomization, Pd(II) (1 mg/mL) was used as modifier while introducing the sample to the graphite tube. Calibration graph was prepared in the range from 10 ng mL-1 to 200 ng mL-1. Samples were suitably diluted to get Se concentration within the linear calibration range. Reagent blanks were prepared along with the samples for blank correction. DSePA concentration was estimated at different time intervals (15 min, 30 min

  18. Paradoxical Increase in 3-Nitropropionic Acid Neurotoxicity by -Phenyl-tert-butylnitrone, a Spin-Trapping Agent.

    Directory of Open Access Journals (Sweden)

    Min-Yu Lan

    2005-02-01

    Full Text Available Background: 3-Nitropropionic acid (3-NP, a mitochondrial toxin, impairs cellular energygeneration by inhibiting succinate dehydrogenase. The basis of its neurotoxicityis oxidative stress in the wake of cellular energy failure. -Phenyl-tertbutyl-nitrone (PBN, a spin-trapping agent with free radical-scavengingcapability, has shown protective effects in various models of experimentalbrain insults. The effect of PBN on the 3-NP neurotoxicity paradigm wasevaluated in this study.Methods: Two groups of adult male mice receiving daily systemic 3-NP administrationwere pretreated with PBN or normal saline respectively for 5 days. After thetreatment course, motor dysfunction and the volume of cerebral lesions werequantitatively evaluated. Cellular apoptosis and expressions of glial fibrillaryacidic protein (GFAP and cyclooxygenase-2 (COX-2 in the brain werecompared between the 2 groups.Results: All mice treated with normal saline and 3-NP survived but developed mildmotor dysfunction. Apoptosis of striatal cells was noted in the absence ofdestructive cerebral lesions. In contrast, combined treatment with PBN and3-NP resulted in more severe motor dysfunction and higher mortality inexperimental animals. Destructive lesions with cellular necrosis, andenhanced expressions of GFAP and COX-2 were noted in the striatum.Conclusions: 3-NP neurotoxicity was paradoxically accentuated by the combined treatmentwith PBN and 3-NP. Metabolic clearance of 3-NP is probably impairedby PBN and the increased oxidative stress caused by higher 3-NP levels mayexceed the free radical-scavenging ability of PBN. The shift from apoptoticto necrotic changes with increased 3-NP toxicity is in accord with the theorythat cellular energy reserves determine the pattern of cellular death.

  19. The effect of dual complexing agents of lactic and citric acids on the formation of sol-gel derived Ag–PbTiO3 percolative thin film

    International Nuclear Information System (INIS)

    Controlling the formation of conductive particles to be nano-scale is important for achieving percolation effect in metal dispersed thin film composite to contribute extraordinary dielectric properties required for miniaturization of electronic devices. In this paper, lactic acid (LA) and citric acid (CA) were used as dual complexing agents to prepare a typical Ag nanoparticle dispersed PbTiO3 (PTO) composite thin film by using a sol-gel method. The phase structure of the thin film and the coordination effect between complexing agent and metallic ions were investigated. It revealed that LA coordinated with Ti4+ and Pb2+ and CA coordinated with Ag+. Lead was fixed inside the gel network by LA and restricted to evaporate during heat treatment thus the pyrochlore phase was prevented from forming in the thin film. Ag+ was coordinated by CA and the diffusion and thus aggregation of silver during gelation and annealing process were weakened. Silver nanoparticles dispersed in the PTO matrix formed with dual complexing agents of LA and CA introduced during the preparation process. The composite thin film of perfect perovskite phase with silver nanoparticles embedded was obtained at the molar ratio of LA/lead = 0.5 and CA/lead = 0.5. The dielectric constant of the thin film with silver nanoparticles is 5 times higher than that without silver nanoparticles. - Highlights: • Ag nanoparticle–PbTiO3 percolative film with high dielectric property is prepared. • Evaporation of lead was prevented by coordinating Pb with lactic acid agent. • Dual complexing agents contribute block and pinning effects to form Ag nanoparticles

  20. Effect of water soluble complexing agent on the extraction of Ce(III) and Nd(III) by 2-ethylhexylphosphonic acid mono-2-ethylhexyl ester

    International Nuclear Information System (INIS)

    Extraction of Ce(III) and Nd(III) by 2-ethylhexylphosphonic acid mono-2-ethylhexyl ester (EHEHPA) in the presence of water soluble complexing agent, glycine, has been studied. An improvement in separation factor between these lanthanides is observed. The extraction data have been analyzed theoretically, taking into account complexation of the metal in the aqueous phase with glycine and chloride ion and plausible complexation in the organic phase. (author) 12 refs.; 4 figs.; 1 tab

  1. α-Linolenic Acid, A Nutraceutical with Pleiotropic Properties That Targets Endogenous Neuroprotective Pathways to Protect against Organophosphate Nerve Agent-Induced Neuropathology

    Directory of Open Access Journals (Sweden)

    Tetsade Piermartiri

    2015-11-01

    Full Text Available α-Linolenic acid (ALA is a nutraceutical found in vegetable products such as flax and walnuts. The pleiotropic properties of ALA target endogenous neuroprotective and neurorestorative pathways in brain and involve the transcription factor nuclear factor kappa B (NF-κB, brain-derived neurotrophic factor (BDNF, a major neuroprotective protein in brain, and downstream signaling pathways likely mediated via activation of TrkB, the cognate receptor of BDNF. In this review, we discuss possible mechanisms of ALA efficacy against the highly toxic OP nerve agent soman. Organophosphate (OP nerve agents are highly toxic chemical warfare agents and a threat to military and civilian populations. Once considered only for battlefield use, these agents are now used by terrorists to inflict mass casualties. OP nerve agents inhibit the critical enzyme acetylcholinesterase (AChE that rapidly leads to a cholinergic crisis involving multiple organs. Status epilepticus results from the excessive accumulation of synaptic acetylcholine which in turn leads to the overactivation of muscarinic receptors; prolonged seizures cause the neuropathology and long-term consequences in survivors. Current countermeasures mitigate symptoms and signs as well as reduce brain damage, but must be given within minutes after exposure to OP nerve agents supporting interest in newer and more effective therapies. The pleiotropic properties of ALA result in a coordinated molecular and cellular program to restore neuronal networks and improve cognitive function in soman-exposed animals. Collectively, ALA should be brought to the clinic to treat the long-term consequences of nerve agents in survivors. ALA may be an effective therapy for other acute and chronic neurodegenerative disorders.

  2. Counteracting foaming caused by lipids or proteins in biogas reactors using rapeseed oil or oleic acid as antifoaming agents

    DEFF Research Database (Denmark)

    Kougias, Panagiotis; Boe, Kanokwan; Einarsdottir, E. S.;

    2015-01-01

    deterioration of the methanogenic process. Many commercial antifoams are derivatives of fatty acids or oils. However, it is well known that lipids can induce foaming in manure based biogas plants. This study aimed to elucidate the effect of rapeseed oil and oleic acid on foam reduction and process performance...... carboxylic ends, is responsible for their foam promoting or foam counteracting behaviour. Thus, it was concluded that the fatty acids and oils could suppress foaming, while salt of fatty acids could generate foam....

  3. Benzyl and Methyl Fatty Hydroxamic Acids Based on Palm Kernel Oil as Chelating Agent for Liquid-Liquid Iron(III Extraction

    Directory of Open Access Journals (Sweden)

    Jamileh Amin

    2012-02-01

    Full Text Available Liquid-liquid iron(III extraction was investigated using benzyl fatty hydroxamic acids (BFHAs and methyl fatty hydroxamic acids (MFHAs as chelating agents through the formation of iron(III methyl fatty hydroxamate (Fe-MFHs or iron(III benzyl fatty hydroxamate (Fe-BFHs in the organic phase. The results obtained under optimized conditions, showed that the chelating agents in hexane extract iron(III at pH 1.9 were realized effectively with a high percentage of extraction (97.2% and 98.1% for MFHAs and BFHAs, respectively. The presence of a large amount of Mg(II, Ni(II, Al(III, Mn(II and Co(II ions did affect the iron(III extraction. Finally stripping studies for recovering iron(III from organic phase (Fe-MFHs or Fe-BFHs dissolved in hexane were carried out at various concentrations of HCl, HNO3 and H2SO4. The results showed that the desired acid for recovery of iron(III was 5 M HCl and quantitative recovery of iron(III was achieved from Fe(III-MFHs and Fe(III-BFHs solutions in hexane containing 5 mg/L of Fe(III.

  4. Biological evaluation of 99mTC cis-Pt iminoacetic acid complexes as tumour imaging agents

    International Nuclear Information System (INIS)

    The biodistributions of three new 99mTc labelled cis-platinum bifunctional tumour imaging agents were examined in mice bearing a certain type of sarcoma between 15 minutes and 24 hours post injection. The three complexes were excreted primarily via the renal pathway into the urine but at quite different rates. All complexes had some affinity for the tumour, but complexes III had the greatest, with tumour to blood and tumour to muscle rates at 24 hours in excess of 10:1 and 18:1. Biodistribution results were calculated using Tiscon Program. Suggesting that the three complexes may be useful as tumour imaging agents. (M.E.L.)

  5. 4-Alkylated homoibotenic acid (HIBO) analogues: versatile pharmacological agents with diverse selectivity profiles towards metabotropic and ionotropic glutamate receptor subtypes

    DEFF Research Database (Denmark)

    Madsen, Ulf; Pickering, Darryl S; Nielsen, Birgitte; Bräuner-Osborne, Hans

    4-Alkylated analogues of homoibotenic acid (HIBO) have previously shown high potency and selectivity at ionotropic and metabotropic glutamic acid receptor (iGluR and mGluR) subtypes. Compounds with different selectivity profiles are valuable pharmacological tools for neuropharmacological studies,...

  6. Identification of retinoic acid in a high content screen for agents that overcome the anti-myogenic effect of TGF-beta-1.

    Directory of Open Access Journals (Sweden)

    Chateen Krueger

    Full Text Available BACKGROUND: Transforming growth factor beta 1 (TGF-β1 is an inhibitor of muscle cell differentiation that is associated with fibrosis, poor regeneration and poor function in some diseases of muscle. When neutralizing antibodies to TGF-β1 or the angiotensin II inhibitor losartan were used to reduce TGF-β1 signaling, muscle morphology and function were restored in mouse models of Marfan Syndrome and muscular dystrophy. The goal of our studies was to identify additional agents that overcome the anti-myogenic effect of TGF-β1. METHODOLOGY/PRINCIPAL FINDINGS: A high-content cell-based assay was developed in a 96-well plate format that detects the expression of myosin heavy chain (MHC in C2C12 cells. The assay was used to quantify the dose-dependent responses of C2C12 cell differentiation to TGF-β1 and to the TGF-β1 Type 1 receptor kinase inhibitor, SB431542. Thirteen agents previously described as promoting C2C12 differentiation in the absence of TGF-β1 were screened in the presence of TGF-β1. Only all-trans retinoic acid and 9-cis retinoic acid allowed a maximal level of C2C12 cell differentiation in the presence of TGF-β1; the angiotensin-converting enzyme inhibitor captopril and 10 nM estrogen provided partial rescue. Vitamin D was a potent inhibitor of retinoic acid-induced myogenesis in the presence of TGF-β1. TGF-β1 inhibits myoblast differentiation through activation of Smad3; however, retinoic acid did not inhibit TGF-β1-induced activation of a Smad3-dependent reporter gene in C2C12 cells. CONCLUSIONS/SIGNIFICANCE: Retinoic acid alleviated the anti-myogenic effect of TGF-β1 by a Smad3-independent mechanism. With regard to the goal of improving muscle regeneration and function in individuals with muscle disease, the identification of retinoic acid is intriguing in that some retinoids are already approved for human therapy. However, retinoids also have well-described adverse effects. The quantitative, high-content assay will be

  7. Investigation of the Prebiotic Synthesis of Amino Acids and RNA Bases from CO2 using FeS/H2S as a Reducing Agent

    Science.gov (United States)

    Keefe, Anthony D.; Miller, Stanley L.; McDonald, Gene; Bada, Jeffrey

    1995-01-01

    An autotrophic theory of the origin of metabolism and life has been proposed in which carbon dioxide is reduced by ferrous sulfide and hydrogen sulfide by means of a reversed citric acid cycle, leading to the production of amino acids. Similar processes have been proposed for purine synthesis. Ferrous sulfide is a strong reducing agent in the presence of hydrogen sulfide and can produce hydrogen as well as reduce alkenes, alkynes, and thiols to saturated hydrocarbons and reduce ketones to thiols. However, the reduction of carbon dioxide has not been demonstrated. We show here that no amino acids, purines, or pyrimidines are produced from carbon dioxide with the ferrous sulfide and hydrogen sulfide system. Furthermore, this system does not produce amino acids from carboxylic acids by reductive amination and carboxylation. Thus, the proposed autotrophic theory, using carbon dioxide, ferrous sulfide, and hydrogen sulfide, lacks the robustness needed to be a geological process and is, therefore, unlikely to have played a role in the origin of metabolism or the origin of life.

  8. In Vitro Dissolution of Fluconazole and Dipyridamole in Gastrointestinal Simulator (GIS), Predicting in Vivo Dissolution and Drug-Drug Interaction Caused by Acid-Reducing Agents.

    Science.gov (United States)

    Matsui, Kazuki; Tsume, Yasuhiro; Amidon, Gregory E; Amidon, Gordon L

    2015-07-01

    Weakly basic drugs typically exhibit pH-dependent solubility in the physiological pH range, displaying supersaturation or precipitation along the gastrointestinal tract. Additionally, their oral bioavailabilities may be affected by coadministration of acid-reducing agents that elevate gastric pH. The purpose of this study was to assess the feasibility of a multicompartmental in vitro dissolution apparatus, Gastrointestinal Simulator (GIS), in predicting in vivo dissolution of certain oral medications. In vitro dissolution studies of fluconazole, a BCS class I, and dipyridamole, a BCS class II weak bases (class IIb), were performed in the GIS as well as United States Pharmacopeia (USP) apparatus II and compared with the results of clinical drug-drug interaction (DDI) studies. In both USP apparatus II and GIS, fluconazole completely dissolved within 60 min regardless of pH, reflecting no DDI between fluconazole and acid-reducing agents in a clinical study. On the other hand, seven-fold and 15-fold higher concentrations of dipyridamole than saturation solubility were observed in the intestinal compartments in GIS with gastric pH 2.0. Precipitation of dipyridamole was also observed in the GIS, and the percentage of dipyridamole in solution was 45.2 ± 7.0%. In GIS with gastric pH 6.0, mimicking the coadministration of acid-reducing agents, the concentration of dipyridamole was equal to its saturation solubility, and the percentage of drug in solution was 9.3 ± 2.7%. These results are consistent with the clinical DDI study of dipyridamole with famotidine, which significantly reduced the Cmax and area under the curve. An In situ mouse infusion study combined with GIS revealed that high concentration of dipyridamole in the GIS enhanced oral drug absorption, which confirmed the supersaturation of dipyridamole. In conclusion, GIS was shown to be a useful apparatus to predict in vivo dissolution for BCS class IIb drugs. PMID:25985298

  9. Targeted LC-MS derivatization for aldehydes and carboxylic acids with a new derivatization agent 4-APEBA

    NARCIS (Netherlands)

    Eggink, M.; Wijtmans, M.; Kretschmer, A.; Kool, J.; Lingeman, H.; Esch, de I.J.P.; Niessen, W.M.A.; Irth, H.

    2010-01-01

    Based on the template of a recently introduced derivatization reagent for aldehydes, 4-(2-(trimethylammonio)ethoxy)benzeneaminium dibromide (4-APC), a new derivatization agent was designed with additional features for the analysis and screening of biomarkers of lipid peroxidation. The new derivatiza

  10. Compatibilization of immiscible poly(lactic acid)/poly(ε-caprolactone) blend through electron-beam irradiation with the addition of a compatibilizing agent

    International Nuclear Information System (INIS)

    The aim of this study was to compatibilize immiscible poly(lactic acid) (PLA)/poly(ε-caprolactone) (PCL) blend by using electron-beam radiation method with the addition of a compatibilizing agent. Glycidyl methacrylate (GMA) was chosen as the compatibilizing agent, in the expectation that the GMA plays a role as a monomeric compatibilizer and a reactive agent at the interface between the PLA and the PCL phases. Compatibilization process has been investigated through the melt mixing of the PLA/PCL and the GMA by using a twin-screw extruder and the exposure of the PLA/PCL/GMA mixture to electron-beam radiation at room temperature. The melt mixing process was performed to locate the GMA at the interface, thereby expecting a finer morphology due to the GMA as the monomeric plasticizer. The exposure process was carried out to induce definite interfacial adhesion at the interface through electron-beam initiated cross-copolymerization by the medium of the GMA as the reactive agent. To investigate the results of this compatibilization strategy, the morphological, mechanical, and rheological properties of the blend were analyzed. The morphological study clearly showed the reduced particle size of dispersed PCL domains and significantly improved interfacial adhesion by the electron-beam irradiation with the addition of the GMA. The stress–strain curves of the blends irradiated at less than 20 kGy showed the typical characteristics of ductile materials. The tensile properties of the blend were strongly affected by the dose of irradiation. - Highlights: ► PLA/PCL blend was compatibilized by the electron-beam irradiation with the addition of GMA. ► GMA played the role of a monomeric compatibilizer and a reactive agent at the interface. ► Definite interfacial adhesion was produced through radiation initiated cross-copolymerization. ► The stress–strain curves of blends irradiated at less than 20 kGy showed a ductile behavior.

  11. In Vivo Performance of a Novel Fluorinated Magnetic Resonance Imaging Agent for Functional Analysis of Bile Acid Transport

    OpenAIRE

    Vivian, Diana; Cheng, Kunrong; Khurana, Sandeep; Xu, Su; Kriel, Edwin H; Dawson, Paul A.; Raufman, Jean-Pierre; Polli, James E.

    2014-01-01

    A novel trifluorinated cholic acid derivative, CA-lys-TFA, was designed and synthesized for use as a tool to measure bile acid transport noninvasively using magnetic resonance imaging (MRI). In the present study, the in vivo performance of CA-lys-TFA for measuring bile acid transport by MRI was investigated in mice. Gallbladder CA-lys-TFA content was quantified using MRI and liquid chromatography/tandem mass spectrometry. Results in wild-type (WT) C57BL/6J mice were compared to those in mice ...

  12. Interfering with the excitatory amino acids signalling in the brain for the design of novel neuroprotective agents

    OpenAIRE

    Vallerini, Gian Paolo

    2013-01-01

    A complex network of central synaptic transmission is regulated, in vertebrates, by simple amino acids: GABA, with inhibitory effects, and glutamate, the most abundant excitatory amino acid in the CNS. These two fundamental neurotransmitters are responsible for the homeostasis of all the CNS functions, from post-natal developmental age to the entire adult life. Even slight dysregulations of GABA-ergic and glutamat-ergic systems underlie the genesis and the progression of a number of neurologi...

  13. New method for studying the efficiency of chelating agents of the polyamine acid series for internal decontamination; Methode nouvelle d'etude de l'efficacite des chelateurs de la serie des acides polyamines pour la decontamination interne

    Energy Technology Data Exchange (ETDEWEB)

    Lafuma, J.; Nenot, J.C.; Morin, M. [Commissariat a l' Energie Atomique, Fontenay-aux-Roses (France). Centre d' Etudes Nucleaires

    1968-07-01

    We followed the biological fate of a complex formed on one side with either a rare earth (cerium-144) or a transuranium element (plutonium-239), and on the other side with a chelating agent of the polyamino acid series (EDTA, BAETA, DTPA, TTHA). This method allowed to study: 1 - the in vivo stability of the various complexes and to compare them; 2 - the stability of the complexes as a function of the isotope - chelating agent weight relationships; 3 - the metabolism of the chelating agents resulting in stable complexes, i. e. DTPA and TTHA mainly. This simple method brought out the higher efficiency, of DTPA in chelating rare earths and plutonium and for therapeutic purposes. (authors) [French] La methode consiste a suivre le devenir biologique d'un complexe forme d'une part avec une terre rare (cerium 144) ou un transuranien (plutonium 239) et d'autre part avec un chelateur de la serie des acides polyamines (EDTA, BAETA, DTPA, TTHA). Elle permet d'etudier: 1 - la stabilite in vivo des differents complexes, de les comparer; 2 - la stabilite des complexes en fonction des rapports ponderaux isotope - chelateurs; 3 - le metabolisme des chelateurs formant des complexes stables, essentiellement DTPA et TTHA. Cette methode simple degage la suprematie du DTPA en ce qui concerne la chelation des terres rares et du plutonium, et son utilisation a des fins therapeutiques. (auteurs)

  14. Targeted LC–MS derivatization for aldehydes and carboxylic acids with a new derivatization agent 4-APEBA

    OpenAIRE

    Eggink, M.; Wijtmans, M; Kretschmer, A.; Kool, J.; Lingeman, H.; Esch, van, H.; Niessen, W.M.A.; Irth, H.

    2010-01-01

    Based on the template of a recently introduced derivatization reagent for aldehydes, 4-(2-(trimethylammonio)ethoxy)benzeneaminium dibromide (4-APC), a new derivatization agent was designed with additional features for the analysis and screening of biomarkers of lipid peroxidation. The new derivatization reagent, 4-(2-((4-bromophenethyl)dimethylammonio)ethoxy)benzenaminium dibromide (4-APEBA) contains a bromophenethyl group to incorporate an isotopic signature to the derivatives and to add add...

  15. The effect of nitrate, bicarbonate and natural organic matter on the degradation of sunscreen agent p-aminobenzoic acid by simulated solar irradiation

    International Nuclear Information System (INIS)

    Our experiments revealed that a model sunscreen agent, p-aminobenzoic acid (PABA), can be effectively transformed through reactions that are mediated by simulated solar irradiation. We systematically explored the effects of nitrate ions, bicarbonate and different types of natural organic matter (NOM) on the degradation of PABA by simulated solar irradiation. Experimental data suggest that these components ubiquitous in nature water have different influence on the rates of the photoinduced removal of PABA. Products were extracted and analyzed using LC/MS and a total of four products probably resulting from ·OH and ·NO2 radicals attack were identified and the possible reaction pathways were proposed. The findings in this study provide useful information for understanding the environmental transformation of sunscreen agent in aquatic system. - Highlights: → In this study, we found that p-aminobenzoic acid (PABA) can be removed by simulated solar irradiation from water. → Influence of environmental components on the photodegradation of PABA was further studied. → We verified using LC/MS that PABA was transformed into four compounds. → We proposed the possible reaction pathways probably resulting from ·OH and ·NO2 radicals attack to PABA.

  16. TAT peptide-based micelle system for potential active targeting of anti-cancer agents to acidic solid tumors

    OpenAIRE

    Sethuraman, Vijay A.; Bae, You Han

    2006-01-01

    A novel drug targeting system for acidic solid tumors has been developed based on ultra pH sensitive polymer and cell penetrating TAT. The delivery system consisted of two components: 1) A polymeric micelle that has a hydrophobic core made of Poly(L-lactic acid) (PLLA) and a hydrophilic shell consisting of Polyethylene Glycol (PEG) conjugated to TAT (TATmicelle), 2) An ultra pH sensitive diblock copolymer of poly(methacryloyl sulfadimethoxine) (PSD) and PEG (PSD-b-PEG). The anionic PSD is com...

  17. Benzene-Poly-Carboxylic Acid Complex, a Novel Anti-Cancer Agent Induces Apoptosis in Human Breast Cancer Cells

    OpenAIRE

    Fares, Fuad; Azzam, Naiel; Fares, Basem; Larsen, Stig; Lindkaer-Jensen, Steen

    2014-01-01

    Some cases of breast cancer are composed of clones of hormonal-independent growing cells, which do not respond to therapy. In the present study, the effect of Benzene-Poly-Carboxylic Acid Complex (BP-C1) on growth of human breast-cancer cells was tested. BP-C1 is a novel anti-cancer complex of benzene-poly-carboxylic acids with a very low concentration of cis-diammineplatinum (II) dichloride. Human breast cancer cells, MCF-7 and T47D, were used. Cell viability was detected by XTT assay and ap...

  18. [Mefenamic acid and other non-steroidal anti-inflammatory agents in dental practice. A review of the literature].

    Science.gov (United States)

    Künzel, André Rätzer; Haschke, Manuel; Surber, Christian; Lambrecht, J Thomas

    2007-01-01

    There are no studies verifying that mefenamic acid is more effective than other NSAID (= non-steroidal anti-inflammatory drugs). However, there are several notions in the literature that this drug is less well-tolerated than other NSAID because over a prolonged period of application more lesions of the upper gastro-intestinal tract are induced as well as occasionally renal insufficiency. Compared to other NSAID the systemic toxicity starts already with relatively low doses above the maximal daily dose. Considering current knowledge there is no reason to prefer mefenamic acid to other NSAID. PMID:17330662

  19. Mycophenolate Antagonizes IFN-γ-Induced Catagen-Like Changes via β-Catenin Activation in Human Dermal Papilla Cells and Hair Follicles

    OpenAIRE

    Sunhyo Ryu; Yonghee Lee; Moo Yeol Hyun; Sun Young Choi; Kwan Ho Jeong; Young Min Park; Hoon Kang; Kui Young Park; Armstrong, Cheryl A.; Andrew Johnson; Peter I. Song; Beom Joon Kim

    2014-01-01

    Recently, various immunosuppressant drugs have been shown to induce hair growth in normal hair as well as in alopecia areata and androgenic alopecia; however, the responsible mechanism has not yet been fully elucidated. In this study, we investigate the influence of mycophenolate (MPA), an immunosuppressant, on the proliferation of human dermal papilla cells (hDPCs) and on the growth of human hair follicles following catagen induction with interferon (IFN)-γ. IFN-γ was found to reduce β-caten...

  20. Amino acid PET tracers are reliable markers of treatment responses to single-agent or combination therapies including temozolomide, interferon-β, and/or bevacizumab for glioblastoma

    International Nuclear Information System (INIS)

    Introduction: We examined whether the amino acid PET tracers, trans-1-amino-3-18F-fluorocyclobutanecarboxylic acid (anti-18F-FACBC) and 11C-methyl-L-methionine (11C-Met), are suitable for detecting early responses to combination therapies including temozolomide (TMZ), interferon-β (IFN), and bevacizumab (Bev) in glioblastoma. Methods: Human glioblastoma U87MG (U87) cells were incubated with low dose TMZ to induce chemoresistance. Both trans-1-amino-3-fluoro-1-14C-cyclobutanecarboxylic acid (anti-14C-FACBC) and 3H-methyl-L-methionine (3H-Met) uptake were quantified using triple-label accumulation assays to examine the relationship between tracer uptake and proliferation (3H-thymidine (TdR) accumulation) in vitro. U87 and U87R (TMZ-resistant subculture) cells were inoculated into the right and left basal ganglia, respectively, of F344/N-rnu rats. The efficacy of single-agent (TMZ, Bev) and combination therapy (TMZ/IFN, TMZ/Bev, TMZ/IFN/Bev) was examined in orthotopic gliomas using MRI, Evans blue extravasation, anti-14C-FACBC, and 3H-Met autoradiography, and MIB-1 immunostaining. Results: TMZ treatment decreased 3H-TdR accumulation and the volume distribution of anti-14C-FACBC and 3H-Met in U87 but not U87R cells. TMZ/IFN combination therapy significantly decreased these parameters in U87R cells; however, Bev had no additional effect in vitro. In vivo, U87R-derived gliomas were observed as equivocal tumors on MRI and T2-high intensity lesions. Bev treatment, either alone or in combination, markedly decreased U87 enhancing lesions. By contrast, autoradiographic images using anti-14C-FACBC and 3H-Met clearly delineated tumor extent, which spread widely beyond T2-high intensity lesions and enhancing lesions. TMZ therapy significantly decreased tracer accumulation and proliferation of U87- but not U87R-derived tumors. TMZ/IFN combination treatment significantly decreased these parameters in U87R tumors, which were further reduced (in both tumor types) by Bev addition

  1. Role of Iron(III)-salen Chloride as Oxidizing Agent with Thiodiglycolic Acid: The Effect of Axial Ligands

    OpenAIRE

    Perumal Subramaniam; Thangadurai Vanitha; Thiruttimuthu Kodispathi; Chandra Raj Shanmuga Sundari

    2014-01-01

    En este trabajo se estudia la sulfoxidación del ácido tio - diglicólico con cloruro de Fe(III)-salen, que actúa como agente oxi - dante en un medio 50% acetonitrilo-agua. Se observa un desplaza - miento importante hacia el rojo del valor del λ max del FeIII-salen en medio acuoso. El estudio cinético espectrofotométrico indica que el [FeIII(salen)]+ es la especie oxidante activa y que se sigue una cinética Michaelis-Menten, con respecto al sustrato. La velocidad de reacción es altamente sensib...

  2. Erythrocyte membrane modifying agents and the inhibition of Plasmodium falciparum growth: structure-activity relationships for betulinic acid analogues.

    Science.gov (United States)

    Ziegler, Hanne L; Franzyk, Henrik; Sairafianpour, Majid; Tabatabai, Mehrnoush; Tehrani, Mahboubeh D; Bagherzadeh, Karim; Hägerstrand, Henry; Staerk, Dan; Jaroszewski, Jerzy W

    2004-01-01

    The natural triterpene betulinic acid and its analogues (betulinic aldehyde, lupeol, betulin, methyl betulinate and betulinic acid amide) caused concentration-dependent alterations of erythrocyte membrane shape towards stomatocytes or echinocytes according to their hydrogen bonding properties. Thus, the analogues with a functional group having a capacity of donating a hydrogen bond (COOH, CH(2)OH, CONH(2)) caused formation of echinocytes, whereas those lacking this ability (CH(3), CHO, COOCH(3)) induced formation of stomatocytes. Both kinds of erythrocyte alterations were prohibitive with respect to Plasmodium falciparum invasion and growth; all compounds were inhibitory with IC(50) values in the range 7-28 microM, and the growth inhibition correlated well with the extent of membrane curvature changes assessed by transmission electron microscopy. Erythrocytes pre-loaded with betulinic acid or its analogues and extensively washed in order to remove excess of the chemicals could not serve as hosts for P. falciparum parasites. Betulinic acid and congeners can be responsible for in vitro antiplasmodial activity of plant extracts, as shown for Zataria multiflora Boiss. (Labiatae) and Zizyphus vulgaris Lam. (Rhamnaceae). The activity is evidently due to the incorporation of the compounds into the lipid bilayer of erythrocytes, and may be caused by modifications of cholesterol-rich membrane rafts, recently shown to play an important role in parasite vacuolization. The established link between erythrocyte membrane modifications and antiplasmodial activity may provide a novel target for potential antimalarial drugs. PMID:14697777

  3. The effect of gamma irradiation on the nitric acid solution as washing agent used in Ru-U extraction process

    International Nuclear Information System (INIS)

    The continuous extraction of uranium was carried out in a 12 -stage bank of mixer-settlers using a 30% volume Tbp-kerosene mixture solvent. The uranyl nitrate solution of 200 g U/l containing 11 mg/l of ruthenium as impurity was fed to the mixer settlers at 7th stage at 75 ml/h flow rate. The 30% volume Tbp-kerosene solvent was introduced at 1st stage at 150 ml/h flow rate, while the nitric acid washing solution already gamma irradiated at 103, 105, 107, 108 rads respectively was fed at 12th stage at 56 ml/h flow rate. Extraction time was 6 hours, and the stirring was done at 2300 rpm. The experiments showed that gamma irradiation caused the degradation of nitric acid which was shown by the decrease in its acidity. Increasing radiation dose to the nitric acid solution resulted in the decrease of uranium recovery and the FDRu-U. At the lowest radiation dose (i.e. 103 rad) the uranium recovery and FDRu-U obtained respectively were found to be 96.37% and 2.19, while that at the highest radiation dose (i.e. 108 rad) they were 88.20% and 2.01 respectively

  4. Counteracting foaming caused by lipids or proteins in biogas reactors using rapeseed oil or oleic acid as antifoaming agents.

    Science.gov (United States)

    Kougias, P G; Boe, K; Einarsdottir, E S; Angelidaki, I

    2015-08-01

    Foaming is one of the major operational problems in biogas plants, and dealing with foaming incidents is still based on empirical practices. Various types of antifoams are used arbitrarily to combat foaming in biogas plants, but without any scientific support this action can lead to serious deterioration of the methanogenic process. Many commercial antifoams are derivatives of fatty acids or oils. However, it is well known that lipids can induce foaming in manure based biogas plants. This study aimed to elucidate the effect of rapeseed oil and oleic acid on foam reduction and process performance in biogas reactors fed with protein or lipid rich substrates. The results showed that both antifoams efficiently suppressed foaming. Moreover rapeseed oil resulted in stimulation of the biogas production. Finally, it was reckoned that the chemical structure of lipids, and more specifically their carboxylic ends, is responsible for their foam promoting or foam counteracting behaviour. Thus, it was concluded that the fatty acids and oils could suppress foaming, while salt of fatty acids could generate foam. PMID:25978353

  5. Ent-trachyloban-19-oic acid isolated from Iostephane heterophylla as a promising antibacterial agent against Streptococcus mutans biofilms.

    Science.gov (United States)

    Hernández, Dulce M; Díaz-Ruiz, Gloria; Rivero-Cruz, Blanca E; Bye, Robert A; Aguilar, María Isabel; Rivero-Cruz, J Fausto

    2012-04-01

    From the roots of Iostephane heterophylla, six known compounds, namely, ent-trachyloban-19-oic acid (1), the mixture of ent-kaur-16-en-19-oic acid (2) and ent-beyer-15-en-19-oic acid (3), xanthorrhizol (4), 16α-hydroxy-ent-kaurane (5) and 16α-hydroxy-ent-kaur-11-en-19-oic acid (6) were isolated using a bioassay-guided fractionation method. The known compounds (1-6) were identified by comparison of their spectroscopic data with reported values in the literature. In an attempt to increase the resultant antimicrobial activity of 1 and 4, a series of reactions was performed on ent-trachyloban-19-oic acid (1) and xanthorrhizol (4), to obtain derivatives 1a, 1b, and 4a-4d. All the isolated compounds (1-6) and the derivatives 1a, 1b, and 4a-4d were evaluated for their antimicrobial activity against two oral pathogens, Streptococcus mutans and Porphyromonas gingivalis associated with caries and periodontal disease, respectively. Compounds 1, 1b, 2+3, 4 and 4d inhibited the growth of S. mutans with concentrations ranging from 4.1 μg/mL to 70.5 μg/mL. No significant activity was found on P. gingivalis except for 4 with an MIC of 6.8 μg/mL. The ability of 1, 1b, 2+3, 4 and 4d to inhibit biofilm formation by S. mutans was evaluated. It was found that 1, 1b, 4 and 4d interfered with the establishment of S. mutans biofilms, inhibiting their development at 32.5, 125.0, 14.1 and 24.4 μg/mL, respectively. PMID:22245083

  6. The role of spices and lactic acid bacteria as antimicrobial agent to extend the shelf life of metata ayib (traditional Ethiopian spiced fermented cottage cheese).

    Science.gov (United States)

    Geremew, Tsehayneh; Kebede, Ameha; Andualem, Berhanu

    2015-09-01

    Spices and lactic acid bacteria have natural antimicrobial substances and organic compounds having antagonistic activity against microorganisms. The objective of this study was to investigate the role of spices and lactic acid bacteria as antimicrobial agent to extend the shelf life of metata ayib. Antimicrobial activities of spices and lactic acid bacteria (LAB) filtrates were determined by agar well diffusion method against E. coli, S. aureus, S. flexneri and S. peumoniae. Aantimicrobial activity of garlic was found to be the most effective against all the tested pathogens. Inhibition zones of garlic extract against all pathogens was significantly (P ≤ 0.05) greater than the remaining spice extracts. Inhibition zones (12.50 ± 1.00 to 15.50 ± 1.00 mm) of ginger and R. graveolens ethanol extracts against all tested pathogens were significantly (P ≤ 0.05) greater than the remaining solvent extracts. Inhibition zone of O. basilicum ethanol extract against all pathogenic bacteria was significantly (p ≤ 0.05) greater than hexane and acetone extracts. Lactobacillus isolates were shown the highest antimicrobial activity than the other LAB isolates against all pathogens. The synergistic effect of spices together with LAB might be contributed a lot to preserve and extend shelf life of metata ayib. Their antimicrobial activity can reduce the risk of spoilage and pathogenesis. The possible reason of LAB isolates was may be due to production of lactic acid, acetic acid and secondary metabolites like bacteriocins. Aseptic processing of traditional cottage cheese (ayib) is by far needed to minimize risks associated during consumption of metata ayib. PMID:26344979

  7. Pulmonary alveolar proteinosis due to mycophenolate and cyclosporine combination therapy in a renal transplant recipient

    OpenAIRE

    Ashfaq Hasan; Raja Ram; TLN Swamy

    2014-01-01

    Pulmonary alveolar proteinosis (PAP) is an orphan disease characterized by the accumulation of excess of surfactant within alveoli and bronchioles. The primary form of PAP (P-PAP; also referred to as idiopathic or autoimmune) is the most common form. It is mediated through a circulating neutralizing antibody against granulocyte-macrophage colony-stimulating factor. Secondary PAP (S-PAP) can be induced by a host of inciting agents and is far more liable to progress to terminal respiratory fail...

  8. Factors involved in the anti-cancer activity of the investigational agents LM985 (flavone acetic acid ester) and LM975 (flavone acetic acid).

    OpenAIRE

    Bibby, M. C.; Double, J A; Phillips, R. M.; Loadman, P.M.

    1987-01-01

    LM985 has been shown previously to hydrolyse to flavone acetic acid (LM975) in mouse plasma and to produce significant anti-tumour effects in transplantable mouse colon tumours (MAC). It has undergone Phase I clinical trials and dose limiting toxicity was acute reversible hypotension. Substantially higher doses of LM975 can be given clinically without dose limiting toxicity. We have investigated the activity of LM975 against a panel of MAC tumours and also the in vitro cytotoxicity of both LM...

  9. Caffeic Acid Phenethyl Ester as a Protective Agent against Nephrotoxicity and/or Oxidative Kidney Damage: A Detailed Systematic Review

    OpenAIRE

    Sumeyya Akyol; Veli Ugurcu; Aynur Altuntas; Rukiye Hasgul; Ozlem Cakmak; Omer Akyol

    2014-01-01

    Caffeic acid phenethyl ester (CAPE), an active component of propolis, has been attracting the attention of different medical and pharmaceutical disciplines in recent years because of its antioxidant, anti-inflammatory, antiproliferative, cytotoxic, antiviral, antifungal, and antineoplastic properties. One of the most studied organs for the effects of CAPE is the kidney, particularly in the capacity of this ester to decrease the nephrotoxicity induced by several drugs and the oxidative injury ...

  10. Molecular Identification of Lactic Acid Bacteria Producing Antimicrobial Agents from Bakasang, An Indonesian Traditional Fermented Fish Product

    OpenAIRE

    Helen Joan Lawalata; Langkah Sembiring; Endang Sutriswati Rahayu

    2015-01-01

    AbstractTwenty seven strains of lactic acid bacteria (LAB) were isolated from bakasang, Indonesian traditional fermented fish product. In general, LAB have inhibitory activity againts pathogenic bacteria and spoilage bacteria. Screening for antimicrobia activity of isolates were performed with well-diffusion method. One isolate that was designed as Pediococcus BksC24 was the strongest against bacteria pathogenic and spoilage bacteria. This strain was further identified by 16S rRNA gen sequenc...

  11. The determination of wear metals in used lubricating oils by flame atomic absorption spectrometry using sulphanilic acid as ashing agent.

    Science.gov (United States)

    Ekanem, E J; Lori, J A; Thomas, S A

    1997-11-01

    A simple and reliable ashing procedure is proposed for the preparation of used lubricating oil samples for the determination of calcium, magnesium, zinc, iron, chromium and nickel by flame atomic absorption spectrometry. Sulphanilic acid was added to oil samples and the mixture coked and the coke ashed at 550 degrees C. The solutions of the ash were analysed by flame AAS for the metals. The release of calcium, zinc, iron and chromium was improved by the addition of sulphanilic acid to samples. The relative standard deviations of metal concentration results in the initial oil samples were 1.5% for Ca (1500 mg l(-1) level), 0.3% for Mg (100 mg l(-1) level), 3.1% for Zn (1500 mg l(-1) level), 0.7% for Fe (500 mg l(-1) level), 0.02% for Cr (50 mg l(-1) level) and 0.002% for Ni (10 mg l(-1) level). The optimum sample size for efficient metal release was 20 g while the optimum sulphanilic acid to oil ratio was 0.05 g per gram of oil for Zn and Cr and 0.10 g for Ca and Fe. Results obtained by this procedure were highly reproducible and comparable with those obtained for the same samples using standard procedures. PMID:18966959

  12. Radiographic scintiscanning agent

    International Nuclear Information System (INIS)

    A new technetium-based scintiscanning agent has been prepared comprising a water soluble sup(99m)Tc-methanehydroxydiphosphonate in combination with a reducing agent selected from stannous, ferrous, chromous and titanous salts. As an additional stabilizer salts and esters of gentisic or ascorbic acids have been used. (E.G.)

  13. Mycophenolate mofetil in low-risk renal transplantation in patients receiving no cyclosporine: a single-centre experience.

    LENUS (Irish Health Repository)

    Raheem, Omer A

    2011-05-28

    BACKGROUND: We assess our long-term experience with regards the safety and efficacy of Mycophenolate Mofetil (MMF) in our low risk renal transplant population and compared it retrospectively to Azathioprine (AZA) immunosuppressive regimen. Patients and methods. Between January 1999 and December 2005, 240 renal transplants received MMF as part of their immunosuppressive protocol (MMF group). AZA group of 135 renal transplants was included for comparative analysis (AZA group). Patients received Cyclosporine was excluded from this study. RESULTS: The incidence of biopsy proven 3-month acute rejections was 30 (12.5%) in MMF group and 22 (16%) in AZA group respectively (P = 0.307). Patient survival rates at 1 and 5 years for the MMF group were 97 and 94%, respectively, compared to 100% and 91% at 1 and 5 years respectively for the AZA group (P = 0.61). Graft survival rates at 1 and 5 years for the MMF group were 95 and 83%, respectively, compared to 97 and 84% at 1 and 5 years, respectively for the AZA group (P = 0.62). CONCLUSION: There was no difference in acute rejection episodes between MMF and AZA based immunotherapy. Additionally, we observed no significant difference concerning graft survival in the MMF group when compared to AZA group.

  14. Mycophenolate mofetil in low-risk renal transplantation in patients receiving no cyclosporine: a single-centre experience.

    LENUS (Irish Health Repository)

    2012-02-01

    BACKGROUND: We assess our long-term experience with regards the safety and efficacy of Mycophenolate Mofetil (MMF) in our low risk renal transplant population and compared it retrospectively to Azathioprine (AZA) immunosuppressive regimen. Patients and methods. Between January 1999 and December 2005, 240 renal transplants received MMF as part of their immunosuppressive protocol (MMF group). AZA group of 135 renal transplants was included for comparative analysis (AZA group). Patients received Cyclosporine was excluded from this study. RESULTS: The incidence of biopsy proven 3-month acute rejections was 30 (12.5%) in MMF group and 22 (16%) in AZA group respectively (P = 0.307). Patient survival rates at 1 and 5 years for the MMF group were 97 and 94%, respectively, compared to 100% and 91% at 1 and 5 years respectively for the AZA group (P = 0.61). Graft survival rates at 1 and 5 years for the MMF group were 95 and 83%, respectively, compared to 97 and 84% at 1 and 5 years, respectively for the AZA group (P = 0.62). CONCLUSION: There was no difference in acute rejection episodes between MMF and AZA based immunotherapy. Additionally, we observed no significant difference concerning graft survival in the MMF group when compared to AZA group.

  15. Caffeic acid phenethyl ester (CAPE) as a remedial agent for reproductive functions and oxidative stress-based pathologies of gonads

    OpenAIRE

    Sumeyya Akyol; Ali Akbas; Ilknur Butun; Muhsin Toktas; Huseyin Ozyurt; Semsettin Sahin; Omer Akyol

    2015-01-01

    In recent years, the studies on the roles of caffeic acid phenethyl ester (CAPE) in several disease models and cell cultures are tremendously growing. It is such a great molecule that was used by ancient times to ameliorate some diseases and nowadays, it is used by modern medicine to test the effectiveness. In this mini-review article, the protection capability of CAPE, as a liposoluble antioxidant and a potent Nuclear Factor kappa B (NF and #954;B) inhibitor, on oxidative and non-oxidative o...

  16. Metal Zn(II), Cu(II), Ni (II) complexes of ursodeoxycholic acid as putative anticancer agents

    OpenAIRE

    Dyakova, Lora; Culita, Daniela-Cristina; Marinescu, Gabriela; Alexandrov, Marin; Kalfin, Reni; Patron, Luminita; Alexandrova, Radostina

    2014-01-01

    The aim of the study was to evaluate the influence of metal [Zn(II), Cu(II), Ni(II)] complexes with ursodeoxycholic acid (UDCA) on the viability and proliferation of tumour and non-tumour cells. Cell lines established from retrovirus-transformed chicken hepatoma (LSCC-SF-Mc29) and rat sarcoma (LSR-SF-SR) as well as from human cancers of the breast (MCF-7), uterine cervix (HeLa), lung (A549) and liver (HepG2) were used as model systems. Non-tumour human embryo (Lep-3) cells were also included ...

  17. Injectable Poly-l-Lactic Acid: A Novel Sculpting Agent for the Treatment of Dermal Fat Atrophy After Severe Acne

    OpenAIRE

    Sadove, Richard

    2008-01-01

    Acne vulgaris affects up to 80% of people 11 to 30 years of age, and scarring can occur for up to 95% of these patients. Scarring may be pitted or hypertrophic in nature, although in most cases it is atrophic. Atrophic acne scarring follows dermal collagen and fat loss after moderate to severe acne infection. Injectable poly-L-acid (PLLA) is a biocompatible, biodegradable, synthetic polymer device that is hypothesized to enhance dermal volume via the endogenous production of fibroblasts and, ...

  18. Synthesis and Conformation of Novel 4'-Fluorinated 5'-Deoxythreosyl Phosphonic Acid Nucleosides as Antiviral Agents

    Energy Technology Data Exchange (ETDEWEB)

    Kang, Lien; Kim, Eunae; Choi, Eun Joo; Yoo, Jin Cheol; Lee, Wonjae; Hong, Joon Hee [Chosun Univ., Kwangju (Korea, Republic of)

    2012-12-15

    Efficient synthetic route to novel 4'-fluorinated 5'-deoxythreosyl phosphonic acid nucleosides was described from glyceraldehyde using Horner-Emmons reaction in the presence of triethyl α-fluorophosphonoacetate. Glycosylation reaction of nucleosidic bases with glycosly donor 14 gave the nucleosides which were further phosphonated and hydrolyzed to reach desired nucleoside analogues. Synthesized nucleoside analogues 18, 21, 25 and 28 were tested for anti-HIV activity as well as cytotoxicity. Adenine derivatives 18 and 21 showed significant anti-HIV activity up to 100 μM.

  19. PREPARATION AND APPLICATION OF COPOLYMERS OF 2-ACRYLAMIDO-2-METHYL PROPANE SULFO ACID AS WASTE WATER TREATMENT AGENTS

    Institute of Scientific and Technical Information of China (English)

    FushanChen; HongjieZhang; HuirenHu; QiushiHe

    2004-01-01

    In this paper, the preparation and application of copolymers of 2-acrylamido-2-methyl propane sulfo acid (AMPS) were discussed. The results showed that the copolymers with molecular weight 18.10 million can be prepared. In treating waste water from deinked pulp, the dosage of copolymers was 0.75ppm, the optimum dosage of PAC was 100ppm; dosage of the amphoteric polyacylamide (AmPAM) with molecular weight 11.34 million was 0.75ppm, the optimum dosage of PAC was 75ppm. Theremoved rate of CODcr was above 70%.

  20. Synthesis and evaluation of single-wall carbon nanotube-paclitaxel-folic acid conjugate as an anti-cancer targeting agent.

    Science.gov (United States)

    Tavakolifard, Sara; Biazar, Esmaeil; Pourshamsian, Khalil; Moslemin, Mohammad H

    2016-08-01

    Single-wall carbon nanotubes (SWCNT) represent a novel nanomaterial applied in various nanotechnology fields because of their surface chemistry properties and high drug cargo capacity. In this study, SWCNT are pre-functionalized covalently with paclitaxel (PTX) - an anticancer drug, and folic acid (FA), as a targeting agent for many tumors. The samples are investigated and evaluated by different analyses such as Fourier transform infrared (FT-IR) spectroscopy, scanning electron microscopy (SEM), thermal gravimetric analysis (TGA), absorption spectroscopic measurements (UV-Visible), elemental analysis, and cell analyses with cancer cell line cultures. The results show good conjugation of the targeting molecule and the anticancer drug on the surface of the carbon nanotubes (CNT). This work demonstrates that the SWCNT-PTX-FA system is a potentially useful system for the targeted delivery of anticancer drugs. PMID:25783856

  1. Synthesis of Caffeic Acid Amides Bearing 2,3,4,5-Tetra-hydrobenzo[b][1,4]dioxocine Moieties and Their Biological Evaluation as Antitumor Agents

    Directory of Open Access Journals (Sweden)

    Ji-Wen Yuan

    2014-06-01

    Full Text Available A series of caffeic acid amides D1-D17 bearing 2,3,4,5-tetrahydrobenzo-[b][1,4]dioxocine units has been synthesized and their biological activities evaluated for potential antiproliferative and EGFR inhibitory activity. Of all the compounds studied, compound D9 showed the most potent inhibitory activity (IC50 = 0.79 μM for HepG2 and IC50 = 0.36 μM for EGFR. The structures of compounds were confirmed by 1H-NMR, ESI-MS and elemental analysis. Among all, the structure of compound D9 ((E-N-(4-ethoxyphenyl-3-(2,3,4,5-tetrahydrobenzo[b][1,4]dioxocin-8-ylacrylamide was also determined by single-crystal X-ray diffraction analysis. Compound D9 was found to be a potential antitumor agent according to biological activity, molecular docking, apoptosis assay and inhibition of HepG2.

  2. Effect of poly-α, γ, L-glutamic acid as a capping agent on morphology and oxidative stress-dependent toxicity of silver nanoparticles

    Directory of Open Access Journals (Sweden)

    Stevanović M

    2011-11-01

    Full Text Available Magdalena Stevanović1, Branimir Kovačević2, Jana Petković3, Metka Filipič3, Dragan Uskoković11Institute of Technical Sciences of Serbian Academy of Sciences and Arts, 2Institute of General and Physical Chemistry, Belgrade, Serbia; 3Department of Genetic Toxicology and Cancer Biology, National Institute of Biology, Ljubljana, SloveniaAbstract: Highly stable dispersions of nanosized silver particles were synthesized using a straightforward, cost-effective, and ecofriendly method. Nontoxic glucose was utilized as a reducing agent and poly- α, γ, L-glutamic acid (PGA, a naturally occurring anionic polymer, was used as a capping agent to protect the silver nanoparticles from agglomeration and render them biocompatible. Use of ammonia during synthesis was avoided. Our study clearly demonstrates how the concentration of the capping agent plays a major role in determining the dimensions, morphology, and stability, as well as toxicity of a silver colloidal solution. Hence, proper optimization is necessary to develop silver colloids of narrow size distribution. The samples were characterized by Fourier transform infrared spectroscopy, ultraviolet-visible spectroscopy, field-emission scanning electron microscopy, transmission electron microscopy, and zeta potential measurement. MTT assay results indicated good biocompatibility of the PGA-capped silver nanoparticles. Formation of intracellular reactive oxygen species was measured spectrophotometrically using 2,7-dichlorofluorescein diacetate as a fluorescent probe, and it was shown that the PGA-capped silver nanoparticles did not induce intracellular formation of reactive oxygen species.Keywords: silver nanoparticles, poly-α, γ, L-glutamic, green synthesis, morphology, cytotoxicity

  3. The outcomes of two different bulking agents (dextranomer hyaluronic acid copolymer and polyacrylate-polyalcohol copolymer in the treatment of primary vesico-ureteral reflux

    Directory of Open Access Journals (Sweden)

    Hakan Taşkinlar

    2016-06-01

    Full Text Available ABSTRACT Purpose Subureteral injection of bulking agents in the endoscopic treatment of vesicoureteral reflux is widely accepted therapy with high success rates. Although the grade of vesicoureteric reflux and experience of surgeon is the mainstay of this success, the characteristics of augmenting substances may have an effect particularly in the long term. In this retrospective study, we aimed to evaluate the clinical outcomes of the endoscopic treatment of vesicoureteric reflux (VUR with two different bulking agents: Dextranomer/hyaluronic acid copolymer (Dx/HA and Polyacrylate polyalcohol copolymer (PPC. Materials and Methods A total 80 patients (49 girls and 31 boys aged 1-12 years (mean age 5.3 years underwent endoscopic subureteral injection for correction of VUR last six years. The patients were assigned to two groups: subureteral injections of Dx/HA (45 patients and 57 ureters and PPC (35 patients and 45 ureters. VUR was grade II in 27 ureters, grade III in 35, grade IV in 22 and grade V in 18 ureters. Results VUR was resolved in 38 (66.6% of 57 ureters and this equates to VUR correction in 33 (73.3% of the 45 patients in Dx/HA group. In PPC group, overall success rate was 88.8% (of 40 in 45 ureters. Thus, Thus, this equates to VUR correction in 31 (88.5% of the 35 patients. Conclusions Our short term data show that two different bulking agent injections provide a high level of reflux resolution and this study revealed that success rate of PPC was significantly higher than Dx/HA with less material.

  4. Benzene-Poly-Carboxylic Acid Complex, a Novel Anti-Cancer Agent Induces Apoptosis in Human Breast Cancer Cells

    Science.gov (United States)

    Fares, Fuad; Azzam, Naiel; Fares, Basem; Larsen, Stig; Lindkaer-Jensen, Steen

    2014-01-01

    Some cases of breast cancer are composed of clones of hormonal-independent growing cells, which do not respond to therapy. In the present study, the effect of Benzene-Poly-Carboxylic Acid Complex (BP-C1) on growth of human breast-cancer cells was tested. BP-C1 is a novel anti-cancer complex of benzene-poly-carboxylic acids with a very low concentration of cis-diammineplatinum (II) dichloride. Human breast cancer cells, MCF-7 and T47D, were used. Cell viability was detected by XTT assay and apoptosis was detected by Flow Cytometry and by annexin V/FITC/PI assay. Caspases were detected by western blot analysis and gene expression was measured by using the Applied Biosystems® TaqMan® Array Plates. The results showed that exposure of the cells to BP-C1 for 48 h, significantly (P<0.001) reduced cell viability, induced apoptosis and activated caspase 8 and caspace 9. Moreover, gene expression experiments indicated that BP-C1 increased the expression of pro-apoptotic genes (CASP8AP1, TNFRSF21, NFkB2, FADD, BCL10 and CASP8) and lowered the level of mRNA transcripts of inhibitory apoptotic genes (BCL2L11, BCL2L2 and XIAP. These findings may lead to the development of new therapeutic strategies for treatment of human cancer using BP-C1 analog. PMID:24523856

  5. Synthesis and biological activities of transition metal complexes based on acetylsalicylic acid as neo-anticancer agents.

    Science.gov (United States)

    Rubner, Gerhard; Bensdorf, Kerstin; Wellner, Anja; Kircher, Brigitte; Bergemann, Silke; Ott, Ingo; Gust, Ronald

    2010-10-14

    [(μ(4)-η(2))-(Prop-2-ynyl)-2-acetoxybenzoate]dicobalthexacarbonyl (Co-ASS), a derivative of aspirin (ASS), demonstrated high growth-inhibitory potential against various tumor cells with interference in the arachidonic acid cascade as probable mode of action. The significance of the kind of metal and cluster was verified in this structure-activity study: Co(2)(CO)(6) was respectively exchanged by a tetrameric cobalt-, trimeric ruthenium-, or trimeric ironcarbonyl cluster. Furthermore, the metal binding motif was changed from alkyne to 1,3-butadiene. Compounds were evaluated for growth inhibition, antiproliferative effects, and apoptosis induction in breast (MCF-7, MDA-MB 231) and colon cancer (HT-29) cell lines and for COX-1/2 inhibitory effects at isolated isoenzymes. Additionally, the major COX metabolite prostaglandin E2 (PGE(2)) was quantified in arachidonic acid-stimulated MDA-MB 231 breast tumor cells. It was demonstrated that the metal cluster was of minor importance for effects on cellular activity if an alkyne was used as ligand. Generally, no correlation existed between growth inhibition and COX activity. Cellular growth inhibition and antiproliferative activity at higher concentrations of the most active compounds Prop-ASS-Co(4) and Prop-ASS-Ru(3) correlated well with apoptosis induction. PMID:20857911

  6. The disulfide compound α-lipoic acid and its derivatives: A novel class of anticancer agents targeting mitochondria.

    Science.gov (United States)

    Dörsam, Bastian; Fahrer, Jörg

    2016-02-01

    The endogenous disulfide α-lipoic acid (LA) is an essential mitochondrial co-factor. In addition, LA and its reduced counterpart dihydro lipoic acid form a potent redox couple with antioxidative functions, for which it is used as dietary supplement and therapeutic. Recently, it has gained attention due to its cytotoxic effects in cancer cells, which is the key aspect of this review. We initially recapitulate the dietary occurrence, gastrointestinal absorption and pharmacokinetics of LA, illustrating its diverse antioxidative mechanisms. We then focus on its mode of action in cancer cells, in which it triggers primarily the mitochondrial pathway of apoptosis, whereas non-transformed primary cells are hardly affected. Furthermore, LA impairs oncogenic signaling and displays anti-metastatic potential. Novel LA derivatives such as CPI-613, which target mitochondrial energy metabolism, are described and recent pre-clinical studies are presented, which demonstrate that LA and its derivatives exert antitumor activity in vivo. Finally, we highlight clinical studies currently performed with the LA analog CPI-613. In summary, LA and its derivatives are promising candidates to complement the arsenal of established anticancer drugs due to their mitochondria-targeted mode of action and non-genotoxic properties. PMID:26604131

  7. Effects of the encapsulation of usnic acid into liposomes and interactions with antituberculous agents against multidrug-resistant tuberculosis clinical isolates

    Directory of Open Access Journals (Sweden)

    Rafaela S Ferraz-Carvalho

    2016-01-01

    Full Text Available Mycobacterium tuberculosis (Mtb has acquired resistance and consequently the antibiotic therapeutic options available against this microorganism are limited. In this scenario, the use of usnic acid (UA, a natural compound, encapsulated into liposomes is proposed as a new approach in multidrug-resistant tuberculosis (MDR-TB therapy. Thus the aim of this study was to evaluate the effect of the encapsulation of UA into liposomes, as well as its combination with antituberculous agents such as rifampicin (RIF and isoniazid (INH against MDR-TB clinical isolates. The in vitro antimycobacterial activity of UA-loaded liposomes (UA-Lipo against MDR-TB was assessed by the microdilution method. The in vitro interaction of UA with antituberculous agents was carried out using checkerboard method. Minimal inhibitory concentration values were 31.25 and 0.98 µg/mL for UA and UA-Lipo, respectively. The results exhibited a synergistic interaction between RIF and UA [fractional inhibitory concentration index (FICI = 0.31] or UA-Lipo (FICI = 0.28. Regarding INH, the combination of UA or UA-Lipo revealed no marked effect (FICI = 1.30-2.50. The UA-Lipo may be used as a dosage form to improve the antimycobacterial activity of RIF, a first-line drug for the treatment of infections caused by Mtb.

  8. On the Use of Molecular Weight Cutoff Cassettes to Measure Dynamic Relaxivity of Novel Gadolinium Contrast Agents: Example Using Hyaluronic Acid Polymer Complexes in Phosphate-Buffered Saline

    Directory of Open Access Journals (Sweden)

    Nima Kasraie

    2011-01-01

    Full Text Available The aims of this study were to determine whether standard extracellular contrast agents of Gd(III ions in combination with a polymeric entity susceptible to hydrolytic degradation over a finite period of time, such as Hyaluronic Acid (HA, have sufficient vascular residence time to obtain comparable vascular imaging to current conventional compounds and to obtain sufficient data to show proof of concept that HA with Gd-DTPA ligands could be useful as vascular imaging agents. We assessed the dynamic relaxivity of the HA bound DTPA compounds using a custom-made phantom, as well as relaxation rates at 10.72 MHz with concentrations ranging between 0.09 and 7.96 mM in phosphate-buffered saline. Linear dependences of static longitudinal relaxation rate (R1 on concentration were found for most measured samples, and the HA samples continued to produce high signal strength after 24 hours after injection into a dialysis cassette at 3T, showing superior dynamic relaxivity values compared to conventional contrast media such as Gd-DTPA-BMA.

  9. On the Use of Molecular Weight Cutoff Cassettes to Measure Dynamic Relaxivity of Novel Gadolinium Contrast Agents: Example Using Hyaluronic Acid Polymer Complexes in Phosphate-Buffered Saline

    International Nuclear Information System (INIS)

    The aims of this study were to determine whether standard extracellular contrast agents of Gd(III) ions in combination with a polymeric entity susceptible to hydrolytic degradation over a finite period of time, such as Hyaluronic Acid (HA), have sufficient vascular residence time to obtain comparable vascular imaging to current conventional compounds and to obtain sufficient data to show proof of concept that HA with Gd-DTPA ligands could be useful as vascular imaging agents. We assessed the dynamic relaxivity of the HA bound DTPA compounds using a custom-made phantom, as well as relaxation rates at 10.72 MHz with concentrations ranging between 0.09 and 7.96 mM in phosphate-buffered saline. Linear dependences of static longitudinal relaxation rate (R1) on concentration were found for most measured samples, and the HA samples continued to produce high signal strength after 24 hours after injection into a dialysis cassette at 3T, showing superior dynamic relaxivity values compared to conventional contrast media such as Gd-DTPA-BMA

  10. Reducing-Agent-Free Instant Synthesis of Carbon-Supported Pd Catalysts in a Green Leidenfrost Droplet Reactor and Catalytic Activity in Formic Acid Dehydrogenation

    Science.gov (United States)

    Lee, Dong-Wook; Jin, Min-Ho; Lee, Young-Joo; Park, Ju-Hyoung; Lee, Chun-Boo; Park, Jong-Soo

    2016-05-01

    The development of green synthesis methods for supported noble metal catalysts remains important challenges to improve their sustainability. Here we first synthesized carbon-supported Pd catalysts in a green Leidenfrost droplet reactor without reducing agents, high-temperature calcination and reduction procedures. When the aqueous solution containing Pd nitrate precursor, carbon support, and water is dripped on a hot plate, vapor layer is formed between a solution droplet and hot surface, which allow the solution droplet to be levitated on the hot surface (Leidenfrost phenomena). Subsequently, Pd nanoparticles can be prepared without reducing agents in a weakly basic droplet reactor created by the Leidenfrost phenomena, and then the as-prepared Pd nanoparticles are loaded on carbon supports during boiling down the droplet on hot surface. Compared to conventional incipient wetness and chemical synthetic methods, the Leidenfrost droplet reactor does not need energy-consuming, time-consuming, and environmentally unfriendly procedures, which leads to much shorter synthesis time, lower carbon dioxide emission, and more ecofriendly process in comparison with conventional synthesis methods. Moreover, the catalysts synthesized in the Leidenfrost droplet reactor provided much better catalytic activity for room-temperature formic acid decomposition than those prepared by the incipient wetness method.

  11. Comparative evaluation of effect of acidic beverage on enamel surface pre-treated with various remineralizing agents: An In vitro study

    Directory of Open Access Journals (Sweden)

    Mithra N Hegde

    2012-01-01

    Full Text Available Aim: This study aimed at quantitatively evaluating the effect of colabased beverage on the calcium loss of enamel surface pre-treated with fluorideenriched casein phosphopeptideamorphous calcium phosphate (CPP-ACPF and βeta-ricalcium phosphate (β-TCP using energy dispersive X-ray analysis (EDX. Materials and Methods: 24 enamel specimens were prepared from the buccal and palatal surfaces of extracted intact human premolars and were randomly assigned to study groups and control group. Specimens of Group II were pre-treated with CPP-ACPF and Group III treated with β-TCP twice daily for 4 for 28 days, followed by storage in artificial saliva. All specimens were evaluated for mineral (calcium and phosphorus content (wt% after pre-treatment using SEM-EDAX. The specimens were then placed in the acidic beverages for 4 days for 10 Mineral content was again measured using SEM-EDAX. Results: Statistical analysis using one-way ANOVA followed by Tukey′s HSD test was applied to compare the re-mineralization and de-mineralization of the samples. Conclusion: The present study concluded that both the remineralizing agents tested were found to be effective in inhibiting the de-mineralization caused by colabased beverage. Among the remineralizing agents tested, β-TCP was found to be more effective than CPP-ACPF.

  12. Effects of the encapsulation of usnic acid into liposomes and interactions with antituberculous agents against multidrug-resistant tuberculosis clinical isolates.

    Science.gov (United States)

    Ferraz-Carvalho, Rafaela S; Pereira, Marcela A; Linhares, Leonardo A; Lira-Nogueira, Mariane Cb; Cavalcanti, Isabella Mf; Santos-Magalhães, Nereide S; Montenegro, Lílian Ml

    2016-05-01

    Mycobacterium tuberculosis (Mtb) has acquired resistance and consequently the antibiotic therapeutic options available against this microorganism are limited. In this scenario, the use of usnic acid (UA), a natural compound, encapsulated into liposomes is proposed as a new approach in multidrug-resistant tuberculosis (MDR-TB) therapy. Thus the aim of this study was to evaluate the effect of the encapsulation of UA into liposomes, as well as its combination with antituberculous agents such as rifampicin (RIF) and isoniazid (INH) against MDR-TB clinical isolates. The in vitro antimycobacterial activity of UA-loaded liposomes (UA-Lipo) against MDR-TB was assessed by the microdilution method. The in vitro interaction of UA with antituberculous agents was carried out using checkerboard method. Minimal inhibitory concentration values were 31.25 and 0.98 µg/mL for UA and UA-Lipo, respectively. The results exhibited a synergistic interaction between RIF and UA [fractional inhibitory concentration index (FICI) = 0.31] or UA-Lipo (FICI = 0.28). Regarding INH, the combination of UA or UA-Lipo revealed no marked effect (FICI = 1.30-2.50). The UA-Lipo may be used as a dosage form to improve the antimycobacterial activity of RIF, a first-line drug for the treatment of infections caused by Mtb. PMID:27143488

  13. Caffeic Acid Phenethyl Ester as a Protective Agent against Nephrotoxicity and/or Oxidative Kidney Damage: A Detailed Systematic Review

    Directory of Open Access Journals (Sweden)

    Sumeyya Akyol

    2014-01-01

    Full Text Available Caffeic acid phenethyl ester (CAPE, an active component of propolis, has been attracting the attention of different medical and pharmaceutical disciplines in recent years because of its antioxidant, anti-inflammatory, antiproliferative, cytotoxic, antiviral, antifungal, and antineoplastic properties. One of the most studied organs for the effects of CAPE is the kidney, particularly in the capacity of this ester to decrease the nephrotoxicity induced by several drugs and the oxidative injury after ischemia/reperfusion (I/R. In this review, we summarized and critically evaluated the current knowledge regarding the protective effect of CAPE in nephrotoxicity induced by several special medicines such as cisplatin, doxorubicin, cyclosporine, gentamycin, methotrexate, and other causes leading to oxidative renal injury, namely, I/R models and senility.

  14. Addictive evaluation of cholic acid-verticinone ester, a potential cough therapeutic agent with agonist action of opioid receptor

    Institute of Scientific and Technical Information of China (English)

    Jiu-liang ZHANG; Hui WANG; Chang CHEN; Hui-fang PI; Han-li RUAN; Peng ZHANG; Ji-zhou WU

    2009-01-01

    Aim: The purpose of this work was to search for potential drugs with potent antitussive and expectorant activities as well as a low toxicity, but without addictive properties. Cholic acid-verticinone ester (CA-Ver) was synthesized based on the clearly elucidated antitussive and expectorant activities of verticinone in bulbs of Fritillaria and different bile acids in Snake Bile. In our previous study, CA-Vet showed a much more potent activity than codeine phosphate. This study was carried out to investigate the central antitussive mechanism and the addictive evaluation of CA-Ver.Methods: Testing on a capsaicin-induced cough model of mice pretreated with naloxone, a non-selective opioid receptor antagonist, was performed for the observation of CA-Ver's central antitussive mechanism. We then took naloxone-induced withdrawal tests of mice for the judgment of CA-Ver's addiction. Lastly, we determined the opioid dependence of CA-Ver in the guinea pig ileum. Results: The test on the capsaicin-induced cough model showed that naloxone could block the antitussive effect of CA-Ver,suggesting the antitussive mechanism of CA-Ver was related to the central opioid receptors. The naloxone-urged withdrawal tests of the mice showed that CA-Ver was not addictive, and the test of the opioid dependence in the guinea pig ileum showed that CA-Ver had no withdrawal response.Conclusion: These findings suggested that CA-Ver deserved attention for its potent antitussive effects related to the central opioid receptors, but without addiction, and had a good development perspective.

  15. Chemical synthesis and characterization of hydroxyapatite (HAp)-poly (ethylene co vinyl alcohol) (EVA) nanocomposite using a phosphonic acid coupling agent for orthopedic applications

    Energy Technology Data Exchange (ETDEWEB)

    Pramanik, Nabakumar; Mohapatra, Sasmita [Department of Chemistry, Indian Institute of Technology Kharagpur, Kharagpur - 721302, West Bengal (India); Bhargava, Parag [Metallurgical Engineering and Materials Science, Indian Institute of Technology Bombay, Mumbai-400076 (India); Pramanik, Panchanan [Department of Chemistry, Indian Institute of Technology Kharagpur, Kharagpur - 721302, West Bengal (India)], E-mail: pramanik@chem.iitkgp.ernet.in

    2009-01-01

    A novel bio-analogue hydroxyapatite (HAp)-poly (ethylene co vinyl alcohol) (EVA) nanocomposite has been synthesized by a solution-based chemical methodology with varying HAp contents from 10 to 60% (w/w). The surface of HAp particles has been modified with 2-carboxyethylphosphonic acid in order to enhance the interfacial bonding interaction between HAp and EVA, and hence to improve the mechanical properties of the composite. The interfacial modification has been investigated through Fourier transform infrared absorption spectra (FTIR), X-ray diffraction (XRD) and thermal analyses. The surface morphology of the composite and the homogeneous dispersion of nanoparticles in the polymer matrix have been investigated through scanning electron microscopy (SEM) and transmission electron microscopy (TEM) respectively. The use of phosphonic acid coupling agent promotes the uniform dispersion of HAp particles in the polymer matrix with strong particle-polymer interfacial bonding, which leads to a significant improvement in mechanical properties of the composite. The cell viability test indicates that the HAp-EVA nanocomposite is cytocompatible. The developed HAp-EVA nanocomposite may be potentially used as bone substitutes.

  16. Chemical synthesis and characterization of hydroxyapatite (HAp)-poly (ethylene co vinyl alcohol) (EVA) nanocomposite using a phosphonic acid coupling agent for orthopedic applications

    International Nuclear Information System (INIS)

    A novel bio-analogue hydroxyapatite (HAp)-poly (ethylene co vinyl alcohol) (EVA) nanocomposite has been synthesized by a solution-based chemical methodology with varying HAp contents from 10 to 60% (w/w). The surface of HAp particles has been modified with 2-carboxyethylphosphonic acid in order to enhance the interfacial bonding interaction between HAp and EVA, and hence to improve the mechanical properties of the composite. The interfacial modification has been investigated through Fourier transform infrared absorption spectra (FTIR), X-ray diffraction (XRD) and thermal analyses. The surface morphology of the composite and the homogeneous dispersion of nanoparticles in the polymer matrix have been investigated through scanning electron microscopy (SEM) and transmission electron microscopy (TEM) respectively. The use of phosphonic acid coupling agent promotes the uniform dispersion of HAp particles in the polymer matrix with strong particle-polymer interfacial bonding, which leads to a significant improvement in mechanical properties of the composite. The cell viability test indicates that the HAp-EVA nanocomposite is cytocompatible. The developed HAp-EVA nanocomposite may be potentially used as bone substitutes

  17. Non-surgical treatment of deep wounds triggered by harmful physical and chemical agents: a successful combined use of collagenase and hyaluronic acid.

    Science.gov (United States)

    Onesti, Maria G; Fino, Pasquale; Ponzo, Ida; Ruggieri, Martina; Scuderi, Nicolò

    2016-02-01

    Some chronic ulcers often occur with slough, not progressing through the normal stages of wound healing. Treatment is long and other therapies need to be performed in addition to surgery. Patients not eligible for surgery because of ASA class (American Society of Anesthesiologists class) appear to benefit from chemical therapy with collagenase or hydrocolloids in order to prepare the wound bed, promoting the healing process. We describe four cases of traumatic, upper limb deep wounds caused by different physical and chemical agents, emphasising the effectiveness of treatment based on topical application of collagenase and hyaluronic acid (HA) before standardised surgical procedures. We performed careful disinfection of lesions combined with application of topical cream containing hyaluronic acid, bacterial fermented sodium hyaluronate (0·2%w/w) salt, and bacterial collagenase obtained from non-pathogenic Vibrio alginolyticus (>2·0 nkat1/g). In one patient a dermo-epidermal graft was used to cover the wide loss of substance. In two patients application of a HA-based dermal substitute was done. We obtained successful results in terms of wound healing, with satisfactory aesthetic result and optimal recovery of the affected limb functionality. Topical application of collagenase and HA, alone or before standardised surgical procedures allows faster wound healing. PMID:24698215

  18. 1-Benzyl-2-methyl-3-indolylmethylene barbituric acid derivatives: Anti-cancer agents that target nucleophosmin 1 (NPM1).

    Science.gov (United States)

    Penthala, Narsimha Reddy; Ketkar, Amit; Sekhar, Konjeti R; Freeman, Michael L; Eoff, Robert L; Balusu, Ramesh; Crooks, Peter A

    2015-11-15

    In the present study, we have designed and synthesized a series of 1-benzyl-2-methyl-3-indolylmethylene barbituric acid analogs (7a-7h) and 1-benzyl-2-methyl-3-indolylmethylene thiobarbituric acid analogs (7 i-7 l) as nucleophosmin 1 (NPM1) inhibitors and have evaluated them for their anti-cancer activity against a panel of 60 different human cancer cell lines. Among these analogs 7 i, 7 j, and 7 k demonstrated potent growth inhibitory effects in various cancer cell types with GI50 values <2 μM. Compound 7 k exhibited growth inhibitory effects on a sub-panel of six leukemia cell lines with GI50 values in the range 0.22-0.35 μM. Analog 7 i also exhibited GI50 values <0.35 μM against three of the leukemia cell lines in the sub-panel. Analogs 7 i, 7 j, 7 k and 7 l were also evaluated against the mutant NPM1 expressing OCI-AML3 cell line and compounds 7 k and 7 l were found to cause dose-dependent apoptosis (AP50 = 1.75 μM and 3.3 μM, respectively). Compound 7k also exhibited potent growth inhibition against a wide variety of solid tumor cell lines: that is, A498 renal cancer (GI50 = 0.19 μM), HOP-92 and NCI-H522 lung cancer (GI50 = 0.25 μM), COLO 205 and HCT-116 colon cancer (GI50 = 0.20 and 0.26 μM, respectively), CNS cancer SF-539 (GI50 = 0.22 μM), melanoma MDA-MB-435 (GI50 = 0.22 μM), and breast cancer HS 578T (GI50 = 0.22 μM) cell lines. Molecular docking studies suggest that compounds 7 k and 7 l exert their anti-leukemic activity by binding to a pocket in the central channel of the NPM1 pentameric structure. These results indicate that the small molecule inhibitors 7 i, 7 j, 7 k, and 7 l could be potentially developed into anti-NPM1 drugs for the treatment of a variety of hematologic malignancies and solid tumors. PMID:26602084

  19. Salicylic acid derivatives as potential anti asthmatic agents using disease responsive drug delivery system for prophylactic therapy of allergic asthma.

    Science.gov (United States)

    Raju, Kalidhindi Rama Satyanarayana; Ambhore, Nilesh S; Mulukutla, Shashank; Gupta, Saurabh; Murthy, Vishakantha; Kumar, M N Kiran; Madhunapantula, Subba Rao V; Kuppuswamy, Gowthamarajan; Elango, Kannan

    2016-02-01

    Asthma is a multi-factorial and complicated lung disorder of the immune system which has expanded to a wider ambit unveiling its etiology to be omnipresent at both ends of the spectrum involving basic pharmacology and in-depth immunology. As asthma occurs through triggered activation of various immune cells due to different stimuli, it poses a great challenge to uncover specific targets for therapeutic interventions. Recent pharmacotherapeutic approaches for asthma have been focused on molecular targeting of transcription factors and their signaling pathways; mainly nucleus factor kappa B (NFκB) and its associated pathways which orchestrate the synthesis of pro-inflammatory cytokines (IL-1β, TNF-α, GM-CSF), chemokines (RANTES, MIP-1a, eotaxin), adhesion molecules (ICAM-1, VCAM-1) and inflammatory enzymes (cyclooxygenase-2 and iNOS). 5-aminosalicylic acid (5-ASA) and sodium salicylate are known to suppress NFκB activation by inhibiting inhibitor of kappa B kinase (IKκB). In order to target the transcription factor, a suitable carrier system for delivering the drug to the intracellular space is essential. 5-ASA and sodium salicylate loaded liposomes incorporated into PEG-4-acrylate and CCRGGC microgels (a polymer formed by crosslinking of trypsin sensitive peptide and PEG-4-acrylate) could probably suit the needs for developing a disease responsive drug delivery system which will serve as a prophylactic therapy for asthmatic patients. PMID:26643666

  20. A prospective multicentre study of mycophenolate mofetil combined with prednisolone as induction therapy in 213 patients with active lupus nephritis.

    Science.gov (United States)

    F, Lu; Y, Tu; X, Peng; L, Wang; H, Wang; Z, Sun; H, Zheng; Z, Hu

    2008-07-01

    Mycophenolate mofetil (MMF) with prednisolone has been associated with high remission rates when used as induction treatment for lupus nephritis. This prospective, multicentre, cohort study investigates the efficacy and safety of this regimen over 24 weeks in 213 Chinese patients with active lupus nephritis (Classes III, IV, V or combination). Baseline activity index (AI) was 6.91+/-3.33 and chronicity index (CI) was 1.9+/-1.2. The remission rate was 82.6% at 24 weeks (complete remission, 34.3%; partial remission, 48.4%). There were significant (P<0.01) improvements in kidney function shown by reductions in proteinuria, serum albumin, serum creatinine and creatinine clearance, as well as in systemic lupus erythematosus disease activity index (SLEDAI) scores. Independent risk factors influencing remission were pathological classification (including Class V and III or Class V and IV nephritis) and elevated serum creatinine at baseline (OR 2.967, 95% CI: 1.479-6.332, P=0.001 and OR 1.007, 95% CI: 1.002-1.011, P=0.001, respectively). Patients with concomitant membranous features on biopsy had a lower remission rate than those with Class III and IV nephritis (66.7% vs 87.3%, P=0.002). Renal biopsy was repeated in 25 patients following treatment. There was a transition to less severe pathological morphologies in majority of subjects. Infections were monitored throughout treatment: eight patients (3.8%) experienced bacterial infections, whereas herpes zoster occurred in seven patients. Nine patients (4.2%) suffered from gastrointestinal upset, which resolved without discontinuation of MMF. One patient became leucopenic, whereas another died from active disease unrelated to kidney symptoms. MMF combined with prednisolone is an effective and well-tolerated induction treatment for patients with active lupus nephritis and for controlling SLE systemic activity. PMID:18625634

  1. Long-term outcome of mycophenolate mofetil treatment for patients with microscopic polyangiitis: an observational study in Chinese patients.

    Science.gov (United States)

    Chen, Yinghua; Gao, Erzhi; Yang, Liu; Liu, Xia; Li, Kang; Liu, Zhengzhao; Zeng, Caihong; Zhang, Haitao; Liu, Zhihong; Hu, Weixin

    2016-07-01

    This study aimed to retrospectively analyze the long-term outcome of mycophenolate mofetil (MMF) therapy for microscopic polyangiitis (MPA) with mild to moderate renal involvement in Chinese patients. Thirty-four MPA patients (24 females, 10 males, aged 44.7 ± 17 years, BVAS score 13.8 ± 3.2, SCr 2.2 ± 1.1 mg/dl) with SCr < 5 mg/dl and who received glucocorticoids plus MMF therapy for inducing and maintaining remission were included in this study. The remission and relapse rates, patient and renal survival rates and adverse events were retrospectively analyzed. We found that 31 (91.2 %) of 34 patients achieved remission and were continuously treated with glucocorticoids plus MMF for maintaining remission. The median duration of MMF treatment was 24 months (IQR 15-53 months) and follow-up time was 86 months (IQR 29-124 months). During the follow-up, 7 (22.6 %) patients relapsed, one patient died, and one patient progressed into end-stage renal disease. The 5-year patient and renal survival rates were 92.8 and 95.2 %, respectively. 11 (32.4 %) patients suffered 16 adverse events, 13 of which were pulmonary infection. In conclusion, glucocorticoids plus MMF regimen as induction and maintenance therapy could achieve high remission rate and good long-term renal survival in MPA patients with mild to moderate renal involvement. Prospective controlled trials with a large sample size are needed to confirm the efficacy of MMF in this population. PMID:27169414

  2. Effect of differentiating agents (all-trans retinoic acid and phorbol 12-myristate 13-acetate on drug sensitivity of HL60 and NB4 cells in vitro.

    Directory of Open Access Journals (Sweden)

    Jadwiga Mirecka

    2008-12-01

    Full Text Available In vitro studies have shown that human myeloid leukemia cell lines: HL60 and NB4 can be stimulated to differentiation by various agents, for example, all-trans retinoic acid (ATRA and phorbol 12-myristate 13-acetate (PMA. The purpose of this study was to investigate whether differentiation of HL60 and NB4 leukemia cell lines induced by ATRA and PMA alters their drug sensitivity. The differentiation along the neutrophil lineage (upon stimulation with ATRA and along the monocyte/macrophage lineage (upon stimulation with PMA was proved by decreased proliferative potential of cells, changes in their morphology, increased ability for NBT reduction and increased expression of CD11b and CD14 cell surface markers. The effect of drugs: cytosine arabinoside, daunorubicin, mitoxantrone and etoposide was examined by Alamar Blue test (proliferation and survival rates, as well as by evaluation of cell smears stained with Hoechst 33342 (apoptotic index. Differentiation resulted in the change of drug sensitivity in both cell lines: the differentiation along the neutrophil pathway (after stimulation with ATRA increased sensitivity to cytosine arabinoside and mitoxantrone but decreased sensitivity to etoposide; the differentiation along the monocyte/macrophage pathway (induced by PMA resulted in the decreased sensitivity of both cell lines to all drugs tested. In conclusion, we have shown that ATRA- and PMA-mediated differentiation of HL60 and NB4 cell lines results in the changes of their drug sensitivity. Our data may provide a contribution to a strategy aimed at a rational combination of differentiating agents and conventional anticancer drugs.

  3. Technetium diagnostic agent and carrier

    International Nuclear Information System (INIS)

    A stable sup(99m)Tc-labelled radioactive diagnostic agent is produced by contacting sup(99m)Tc-containing pertechnetate with a non-radioactive carrier comprising a chelating agent, a water-soluble reducing agent and a stabilizer. The stabilizer is chosen from ascorbic acid and erythorbic acid and their pharmaceutically acceptable salts and esters. A mole ratio of more than 100 moles ascorbic or erythorbic acid to 1 mole of reducing agent provides a stable composition at high levels of radioactivity

  4. Mode of action and resistance studies unveil new roles for tropodithietic acid as an anticancer agent and the γ-glutamyl cycle as a proton sink.

    Science.gov (United States)

    Wilson, Maxwell Z; Wang, Rurun; Gitai, Zemer; Seyedsayamdost, Mohammad R

    2016-02-01

    While we have come to appreciate the architectural complexity of microbially synthesized secondary metabolites, far less attention has been paid to linking their structural features with possible modes of action. This is certainly the case with tropodithietic acid (TDA), a broad-spectrum antibiotic generated by marine bacteria that engage in dynamic symbioses with microscopic algae. TDA promotes algal health by killing unwanted marine pathogens; however, its mode of action (MoA) and significance for the survival of an algal-bacterial miniecosystem remains unknown. Using cytological profiling, we herein determine the MoA of TDA and surprisingly find that it acts by a mechanism similar to polyether antibiotics, which are structurally highly divergent. We show that like polyether drugs, TDA collapses the proton motive force by a proton antiport mechanism, in which extracellular protons are exchanged for cytoplasmic cations. The α-carboxy-tropone substructure is ideal for this purpose as the proton can be carried on the carboxyl group, whereas the basicity of the tropylium ion facilitates cation export. Based on similarities to polyether anticancer agents we have further examined TDA's cytotoxicity and find it to exhibit potent, broad-spectrum anticancer activities. These results highlight the power of MoA-profiling technologies in repurposing old drugs for new targets. In addition, we identify an operon that confers TDA resistance to the producing marine bacteria. Bioinformatic and biochemical analyses of these genes lead to a previously unknown metabolic link between TDA/acid resistance and the γ-glutamyl cycle. The implications of this resistance mechanism in the context of the algal-bacterial symbiosis are discussed. PMID:26802120

  5. All-trans retinoic acid as a single agent induces complete remission in a patient with acute leukemia of M2a subtype

    Institute of Scientific and Technical Information of China (English)

    陈子兴; 王阳; 王玮; 贡静霞; 薛永权

    2002-01-01

    Objective To present a special case with the karyotype and molecular marker of acute myeloid leukemia (AML)-M2 who was induced to complete remission by all-trans retinoic acid (ATRA) alone.Methods A recently hospitalized young female patient with acute leukemia was initially diagnosed as M3 subtype based on morphological French-American-British (FAB) classification. Karyotype analysis using standard G and R banding techniques and RT-PCR were applied to further define the diagnosis. After primarily cultured bone marrow cells from the iliac aspiration were tested for in vitro induced differentiation, the patient was treated with oral all-trans retinoic acid alone, 60?mg per day until complete remission was achieved. Peripheral blood and bone marrow changes were monitored over the whole treatment course.Results The characteristic chromosomal aberration for M3, the t(15;17) reciprocal translocation, was not found while a t(8;21) translocation was verified. Furthermore, an amplified product of the AML-1/ETO fusion gene instead of the PML/RARα fusion gene was detected by RT-PCR and the diagnosis was corrected from M3 to M2. Primary cultured bone marrow cells can be fully induced to terminal differentiation after 4 days exposure to ATRA. A hematological complete remission was achieved after 40 days treatment with ATRA as a single therapeutic agent, suggesting an alternative pathway mediating ATRA-induced myeloid differentiation. Conclusion A leukemia patient with a subtype other than M3, such as M2 in this case, may also be induced to complete remission by the mechanism of ATRA-induced terminal differentiation. This implies that there may be a pathway other than PML/RARα fusion gene product which mediates ATRA-induced myeloid maturation in leukemia cells.

  6. Comparison of pharmacokinetics and clinical application in patients given enteric-coated mycophenolate sodium or mycophenolate mofetil after renal transplantation%肾移植受者口服吗替麦考酚酯和麦考酚钠肠溶片的临床研究

    Institute of Scientific and Technical Information of China (English)

    张希诺; 李寒; 王玮; 张征; 尹航; 邱葵; 刘航; 王伟; 胡小鹏

    2014-01-01

    Objective To evaluate the efficacy and safety of the enteric-coated mycophenolate sodium (EC-MPS) and mycophenolate mofetil (MMF) by pharmacokinetic characteristics after taking the drug.Method 102 renal transplantation recipients were divided into EC-MPS group and MMF group with random number table.Ten limited sampling strategies were used to determine area under the curve (AUC) 0-12 h of mycophenolic acid (MPA) 7 and 30 days after transplantation.Gastrointestinal Symptom Rating Scale (GSRS) was used to assess symptoms of adverse reactions in patients after treatment,and the higher the score,the more obvious symptoms.Simultaneously,rejection rate in both groups was compared.Result There was no significant difference between the two groups in age,sex,weight,cold ischemia time,HLA matching between donor and recipient type,panel reactive antibody (PRA) and viral infections.Seven days after transplantation,the mean time to reach peak (Tmax) in MMF group was significantly shorter than EC-MPS group (1.18 ± 0.97 h vs.2.76 ± 1.35 h,P =0.00).MPA-AUC0-12h of two groups was similar (48.48 ± 7.65 vs.52.39 ± 5.93 mg· h · L-1,P =0.062) ; during 7 days the rejection rate showed no significant difference between two groups (2.00% vs.1.96%,P =0.978).Thirty days after transplantation,the Tmax of MMF group was still shorter than that of EC-MPS group (1.09 ± 0.91 h vs.3.11 ± 1.43 h,P =0.00).MPA-AUC0-12hof MMF group was lower than EC-MPS group (41.96 ± 6.39 vs.50.66 ± 4.21 mg·h· L-1,P =0.00).Although there was no significant difference between two groups in rejection rate,the rejection rate in MMF group was slightly higher than in EC-MPS group (16.0% vs.7.7%,P =0.193) during the 30 days after renal transplantation.Conclusion Tmax was significantly shorter,and MPA-AUC0-12h higher in MMF group than in EC-MPS group.EC-MPS drugs reduced gastrointestinal adverse reactions of MPA.%目的 探讨口服吗替麦考酚酯(MMF)和麦考酚钠肠溶片(EC-MPS)在肾移植患

  7. Alpha-picolinic acid,a fungal toxin and mammal apoptosis-inducing agent,elicits hypersensitive-like response and enhances disease resistance in rice

    Institute of Scientific and Technical Information of China (English)

    Hai Kuo ZHANG; Xin ZHANG; Bi Zeng MAO; Qun LI; Zu Hua HE

    2004-01-01

    Alpha-picolinic acid (PA),a metabolite of tryptophan and an inducer of apoptosis in the animal cell,has been reported to be a toxin produced by some of plant fungal pathogens and used in screening for disease resistant mutants. Here,we report that PA is an efficient apoptosis agent triggering cell death of hypersensitive-like response in planta. Confirmed by Fluorescence Activated Cell Sorter (FACS),rice suspension cells and leaves exhibited programmed cell death induced by PA. The PA-induced cell death was associated with the accumulation of reactive oxygen species that could be blocked by diphenylene iodonium chloride,indicating that the generation of reactive oxygen species was NADPHoxidase dependent. We also demonstrated the induction of rice defense-related genes and subsequent resistant enhancement by PA against the rice blast fungus Magnaporthe grisea. Hence,it was concluded that the PA-stimulated defense response likely involves the onset of the hypersensitive response in rice,which also provides a simple eliciting tool for studying apoptosis in the plant cell.

  8. Repositioning of 2,4-dichlorophenoxy acetic acid as a potential anti-inflammatory agent: in silico and pharmaceutical formulation study.

    Science.gov (United States)

    Khedr, Mohammed A; Shehata, Tamer M; Mohamed, Maged E

    2014-12-18

    2,4-Dichlorophenoxy acetic acid (2,4-D) is a well-known plant auxin which is widely used in plant tissue culture experiments as well as a weed killer and a herbicide. In this study, 2,4-D was rediscovered as a new anti-inflammatory agent through an in silico molecular modeling and docking studies along with drug formulation and in vivo anti-inflammatory inspection. The molecular modeling and docking studies indicated high affinity of 2,4-D toward COX-2 enzyme in a way similar to Ibuprofen, suggesting a higher anti-inflammatory activity. Molecular docking by both MOE 2013.08 and Leadit 2.1.2 revealed excellent binding pattern compared to some of well-known non-steroidal anti-inflammatory drugs. 2,4-D was formulated in different gel bases. In vitro drug release experiments were used to examine the best 2,4-D formula for in vivo studies. In vivo carrageenan-induced hind paw edema inflammatory model in rats was used to test the in silico finding. 2,4-D showed potential in vivo anti-inflammatory activity and significantly reduced the concentration of prostaglandin E2 in hind paw tissues in a way similar to Ibuprofen. These results may open the door to introduce a new anti-inflammatory molecule; especially that 2,4-D is a well-investigated regarding its toxicity and side effect. PMID:25245006

  9. Oxyresveratrol and ascorbic acid O/W microemulsion: Preparation, characterization, anti-isomerization and potential application as antibrowning agent on fresh-cut lotus root slices.

    Science.gov (United States)

    He, Jianfei; Zhu, Qin; Dong, Xue; Pan, Hongyang; Chen, Jie; Zheng, Zong-Ping

    2017-01-01

    The purpose of this study is to prepare an oxyresveratrol (Oxy) microemulsion (ME) with improved Oxy's solubility and stability and to investigate its antibrowning effects on fresh-cut lotus root slices. The formula of OxyME consisted of ethyl butyrate, Tween 80, PEG400, and water with w/w of 4%, 10.67%, 5.33%, and 80%, respectively. Encapsulating Oxy into OxyME greatly increased its solubility and stability compared with that of in water. Strong antibrowning effects were observed on fresh-cut lotus root slices treated with OxyME, even better than 4-hexylresorcinol. The addition of ascorbic acid (VC) into OxyME greatly improved the Oxy stability in long-term storage and antibrowning effects on fresh-cut lotus root slices. However, the simultaneous addition of calcium chloride and VC did not obviously improve the antibrowning effects compared with the addition of VC alone. These results indicated that Oxy+VCME may be suitable as an antibrowning agent for fresh-cut vegetables. PMID:27507475

  10. 3-Bromopyruvic acid, a hexokinase II inhibitor, is an effective antitumor agent on the hepatoma cells : in vitro and in vivo findings.

    Science.gov (United States)

    Gong, Lei; Wei, Yuhua; Yu, Xin; Peng, Jirun; Leng, Xisheng

    2014-06-01

    Over-expressed in cancer cells, hexokinase II (HK II) forms a mitochondrial complex, which promotes cancer survival. 3- Bromopyruvic acid (3-BrPA) dissociates HK II from this complex, causing cell death, and thus, having an anti-tumor effect. The design of this study was to first analyze the expression of HK II in the hepatoma cell line, BEL-7402, then investigate the effects of 3-Br-PA on these cells, and finally, discuss its potential for clinical usage. HK II expression was detected in BEL-7402 cells by immunocytochemistry and reverse transcriptase polymerase chain reaction (RT-PCR). In vitro treatment of cells with 3-BrPA significantly inhibited their growth, as evaluated by MTT assay and adenosine triphosphate-tumor chemosensitivity assay (ATP-TCA). To analyze the in vivo function and safety of this drug, a tumor model was established by subcutaneously implanting hepatic cancer cells into nude mice. 3-BrPA treatment (50 mg/kg ip. daily, 6 days/week for three weeks) was effective in the animal model by attenuating tumor growth and causing tumor necrosis. Toxic signs were not observed. The acute toxicity study provided an LD50 of 191.7 mg/kg for 3-BrPA. Taken together, our in vitro and in vivo analyses suggest that 3-BrPA exerts anti-hepatoma effects, and may be an effective pharmacological agent for the treatment of hepatocellular carcinoma. PMID:24738957

  11. Capillary Electrophoresis for the Simultaneous Determination of Metals by Using Ethylenediamine Tetraacetic Acid as Complexing Agent and Vancomycin as Complex Selector

    Institute of Scientific and Technical Information of China (English)

    THREEPROM, Jirasak; SOM-AUM, Waraporn; LIN, Jin-Ming

    2006-01-01

    A new separation system of capillary electrophoresis for the simultaneous determination of metals by using ethylenediamine tetraacetic acid (EDTA) as complexing agent and employing vancomycin as complex selector was described. The Z-shape cell capillary electrophoresis was used to enhance the sensitivity for the determination of the complexes of Cu(Ⅱ), Ni(Ⅱ), Co(Ⅱ) and Fe(Ⅲ) with EDTA. The partial filling method (co-current mode) was used in order to increase the selectivity of the electrophoretic method, meanwhile vancomycin was not present at the detector path during the detection of metal-EDTA complexes. The vancomycin concentration, phosphate concentration and pH of the buffer strongly influenced mobility, resolution and selectivity of the studied analytes. Under the optimal condition, the relative standard deviations (n=5) of the migration time and the peak area were less than 3.14% and 7.35%, respectively. Application of the Z-shape cell capillary electrophoresis method with UV detection and vancomycin loading led to the reliable determination of these metal ions in tap water and the recoveries were 97%-101%. The detection limits based on a signal to noise ratio of 3: 1 were found in the range of 2-10 μg·L-1.

  12. Oral nimodipine reduces prostaglandin and thromboxane production by arteries chronically exposed to a periarterial haematoma and the antifibrinolytic agent tranexamic acid.

    Science.gov (United States)

    Pickard, J D; Walker, V; Vile, J; Perry, S; Smythe, P J; Hunt, R

    1987-06-01

    The calcium antagonist nimodipine blocks the effects of many vasoconstrictors of cerebrovascular smooth muscle and may reduce the incidence of delayed cerebral ischaemia following subarachnoid haemorrhage though not necessarily by inhibiting the development of angiographic cerebral vasospasm. Post-haemorrhagic CSF contains abnormally large quantities of various eicosanoids that partly reflect enhanced production by cerebral arteries. Does nimodipine affect this process? The extra-arterial and intra-arterial production of PG6 keto-F1 alpha, PGE2, PGF2 alpha and TXB2 were measured in perfused common carotid arteries taken from rabbits in which the arteries had been ensheathed by blood clot in vivo for 7 days. All rabbits were given the antifibrinolytic agent tranexamic acid to retard resolution of the clot, and half were given oral nimodipine (2 mg/kg/day) for 10 days. Nimodipine significantly reduced the extra-arterial production of TXB2 during the third and fourth hours of perfusion and, less consistently, the production of PGF2 alpha, PGE2 and PG6 keto-F1 alpha. Lutrol, the solvent for nimodipine, had no such effect. PMID:3475405

  13. Adrenal imaging agents

    International Nuclear Information System (INIS)

    The goals of this proposal are the development of selenium-containing analogs of the aromatic amino acids as imaging agents for the pancreas and of the adrenal cortex enzyme inhibitors as imaging agents for adrenal pathology. The objects for this year include (a) the synthesis of methylseleno derivatives of phenylalanine and tryptophan, and (b) the preparation and evaluation of radiolabeled iodobenzoyl derivatives of the selenazole and thiazole analogs of metyrapone and SU-9055

  14. Mycophenolate mofetil modulates adhesion receptors of the beta1 integrin family on tumor cells: impact on tumor recurrence and malignancy

    Directory of Open Access Journals (Sweden)

    Beecken Wolf-Dietrich

    2005-01-01

    Full Text Available Abstract Background Tumor development remains one of the major obstacles following organ transplantation. Immunosuppressive drugs such as cyclosporine and tacrolimus directly contribute to enhanced malignancy, whereas the influence of the novel compound mycophenolate mofetil (MMF on tumor cell dissemination has not been explored. We therefore investigated the adhesion capacity of colon, pancreas, prostate and kidney carcinoma cell lines to endothelium, as well as their beta1 integrin expression profile before and after MMF treatment. Methods Tumor cell adhesion to endothelial cell monolayers was evaluated in the presence of 0.1 and 1 μM MMF and compared to unstimulated controls. beta1 integrin analysis included alpha1beta1 (CD49a, alpha2beta1 (CD49b, alpha3beta1 (CD49c, alpha4beta1 (CD49d, alpha5beta1 (CD49e, and alpha6beta1 (CD49f receptors, and was carried out by reverse transcriptase-polymerase chain reaction, confocal microscopy and flow cytometry. Results Adhesion of the colon carcinoma cell line HT-29 was strongly reduced in the presence of 0.1 μM MMF. This effect was accompanied by down-regulation of alpha3beta1 and alpha6beta1 surface expression and of alpha3beta1 and alpha6beta1 coding mRNA. Adhesion of the prostate tumor cell line DU-145 was blocked dose-dependently by MMF. In contrast to MMF's effects on HT-29 cells, MMF dose-dependently up-regulated alpha1beta1, alpha2beta1, alpha3beta1, and alpha5beta1 on DU-145 tumor cell membranes. Conclusion We conclude that MMF possesses distinct anti-tumoral properties, particularly in colon and prostate carcinoma cells. Adhesion blockage of HT-29 cells was due to the loss of alpha3beta1 and alpha6beta1 surface expression, which might contribute to a reduced invasive behaviour of this tumor entity. The enhancement of integrin beta1 subtypes observed in DU-145 cells possibly causes re-differentiation towards a low-invasive phenotype.

  15. Mycophenolate mofetil modulates adhesion receptors of the beta1 integrin family on tumor cells: impact on tumor recurrence and malignancy

    International Nuclear Information System (INIS)

    Tumor development remains one of the major obstacles following organ transplantation. Immunosuppressive drugs such as cyclosporine and tacrolimus directly contribute to enhanced malignancy, whereas the influence of the novel compound mycophenolate mofetil (MMF) on tumor cell dissemination has not been explored. We therefore investigated the adhesion capacity of colon, pancreas, prostate and kidney carcinoma cell lines to endothelium, as well as their beta1 integrin expression profile before and after MMF treatment. Tumor cell adhesion to endothelial cell monolayers was evaluated in the presence of 0.1 and 1 μM MMF and compared to unstimulated controls. beta1 integrin analysis included alpha1beta1 (CD49a), alpha2beta1 (CD49b), alpha3beta1 (CD49c), alpha4beta1 (CD49d), alpha5beta1 (CD49e), and alpha6beta1 (CD49f) receptors, and was carried out by reverse transcriptase-polymerase chain reaction, confocal microscopy and flow cytometry. Adhesion of the colon carcinoma cell line HT-29 was strongly reduced in the presence of 0.1 μM MMF. This effect was accompanied by down-regulation of alpha3beta1 and alpha6beta1 surface expression and of alpha3beta1 and alpha6beta1 coding mRNA. Adhesion of the prostate tumor cell line DU-145 was blocked dose-dependently by MMF. In contrast to MMF's effects on HT-29 cells, MMF dose-dependently up-regulated alpha1beta1, alpha2beta1, alpha3beta1, and alpha5beta1 on DU-145 tumor cell membranes. We conclude that MMF possesses distinct anti-tumoral properties, particularly in colon and prostate carcinoma cells. Adhesion blockage of HT-29 cells was due to the loss of alpha3beta1 and alpha6beta1 surface expression, which might contribute to a reduced invasive behaviour of this tumor entity. The enhancement of integrin beta1 subtypes observed in DU-145 cells possibly causes re-differentiation towards a low-invasive phenotype

  16. Dosing of Enteric-Coated Mycophenolate Sodium Under Routine Conditions: An Observational, Multicenter Study in Kidney Transplantation.

    Science.gov (United States)

    Albano, Laetitia; Buchler, Matthias; Cantarovich, Diego; Cassuto, Elisabeth; Cointault, Olivier; Mazouz, Hakim; Vetromile, Fernando; Lecuyer, Aurélie; Tindel, Malka; Kamar, Nassim

    2016-01-01

    BACKGROUND Dosing of enteric-coated mycophenolate sodium (EC-MPS) should be adjusted to reflect concomitant immunosuppression, but it is largely undocumented whether such modifications are carried out during routine clinical practice. MATERIAL AND METHODS MyLIFE was an observational study of adult kidney-only or kidney-pancreas transplant patients starting -EC-MPS at 33 French transplant centers. Data were collected at first EC-MPS dose and 6 months later. The primary objective was to describe initial EC-MPS dosing according to concomitant immunosuppression. RESULTS There were 461 patients analyzed (174 started EC-MPS by month 1 post-transplant ['de novo'] and 287 started EC-MPS >1 month post-transplant ['maintenance']), receiving cyclosporine (CsA) (n=76), tacrolimus (n=363), or a mammalian target of rapamycin (mTOR) inhibitor (n=22). Mean (SD) starting dose was 1130 (511) mg/day, 1006 (441) mg/day, and 769 (300) mg/day in the CsA, tacrolimus, and mTOR inhibitor groups, respectively (p=0.003). In the de novo subpopulation, the starting dose was 1440 mg/day in 66.7% (14/21) of CsA-treated patients and 71.9% (110/153) of tacrolimus-treated patients, with an intensified dose of 2160 mg/day in 28.6% (6/21) and 8.5% (13/153), respectively. There was a non-significant trend to a higher rate of biopsy-proven acute rejection in patients receiving CsA versus tacrolimus or an mTOR inhibitor (p=0.082). Adverse events with a suspected relation to EC-MPS occurred in 21.0%, 23.1%, and 9.1% of the CsA, tacrolimus, and mTOR inhibitor subpopulations, respectively. CONCLUSIONS EC-MPS is usually initiated at the dose recommended for de novo CsA-treated kidney transplant patients, then titrated downwards as required. An early intensified regimen is not used frequently. The EC-MPS dose is modified in <20% of de novo patients to account for concomitant tacrolimus therapy instead of CsA administration. PMID:27122116

  17. Eicosapentaenoic Acid Inhibits Oxidation of ApoB-containing Lipoprotein Particles of Different Size In Vitro When Administered Alone or in Combination With Atorvastatin Active Metabolite Compared With Other Triglyceride-lowering Agents.

    Science.gov (United States)

    Mason, R Preston; Sherratt, Samuel C R; Jacob, Robert F

    2016-07-01

    Eicosapentaenoic acid (EPA) is a triglyceride-lowering agent that reduces circulating levels of the apolipoprotein B (apoB)-containing lipoprotein particles small dense low-density lipoprotein (sdLDL), very-low-density lipoprotein (VLDL), and oxidized low-density lipoprotein (LDL). These benefits may result from the direct antioxidant effects of EPA. To investigate this potential mechanism, these particles were isolated from human plasma, preincubated with EPA in the absence or presence of atorvastatin (active) metabolite, and subjected to copper-initiated oxidation. Lipid oxidation was measured as a function of thiobarbituric acid reactive substances formation. EPA inhibited sdLDL (IC50 ∼2.0 μM) and LDL oxidation (IC50 ∼2.5 μM) in a dose-dependent manner. Greater antioxidant potency was observed for EPA in VLDL. EPA inhibition was enhanced when combined with atorvastatin metabolite at low equimolar concentrations. Other triglyceride-lowering agents (fenofibrate, niacin, and gemfibrozil) and vitamin E did not significantly affect sdLDL, LDL, or VLDL oxidation compared with vehicle-treated controls. Docosahexaenoic acid was also found to inhibit oxidation in these particles but over a shorter time period than EPA. These data support recent clinical findings and suggest that EPA has direct antioxidant benefits in various apoB-containing subfractions that are more pronounced than those of other triglyceride-lowering agents and docosahexaenoic acid. PMID:26945158

  18. D-amino acid peptide residualizing agents bearing N-hydroxysuccinimido- and maleimido-functional groups and their application for trastuzumab radioiodination

    International Nuclear Information System (INIS)

    Introduction: Proteins that undergo receptor-mediated endocytosis are subject to lysosomal degradation, requiring radioiodination methods that minimize loss of radioactivity from tumor cells after this process occurs. To accomplish this, we developed the residualizing radioiodination agent Nϵ-(3-[⁎I]iodobenzoyl)-Lys5-Nα-maleimido-Gly1-D-GEEEK (Mal-D-GEEEK-[⁎I]IB), which enhanced tumor uptake but also increased kidney activity and necessitates generation of sulfhydryl moieties on the protein. The purpose of the current study was to synthesize and evaluate a new D-amino acid based agent that might avoid these potential problems. Methods: Nα-(3-iodobenzoyl)-(5-succinimidyloxycarbonyl)-D-EEEG (NHS-IB-D-EEEG), which contains 3 D-glutamates to provide negative charge and a N-hydroxysuccinimide function to permit conjugation to unmodified proteins, and the corresponding tin precursor were produced by solid phase peptide synthesis and subsequent conjugation with appropriate reagents. Radioiodination of the anti-HER2 antibody trastuzumab using NHS-IB-D-EEEG and Mal-D-GEEEK-IB was compared. Paired-label internalization assays on BT474 breast carcinoma cells and biodistribution studies in athymic mice bearing BT474M1 xenografts were performed to evaluate the two radioiodinated D-peptide trastuzumab conjugates. Results: NHS-[131I]IB-D-EEEG was produced in 53.8% ± 13.4% and conjugated to trastuzumab in 39.5% ± 7.6% yield. Paired-label internalization assays with trastuzumab-NHS-[131I]IB-D-EEEG and trastuzumab-Mal-D-GEEEK-[125I]IB demonstrated similar intracellular trapping for both conjugates at 1 h (131I, 84.4% ± 6.1%; 125I, 88.6% ± 5.2%) through 24 h (131I, 60.7% ± 6.8%; 125I, 64.9% ± 6.9%). In the biodistribution experiment, tumor uptake peaked at 48 h (trastuzumab-NHS-[131I]IB-D-EEEG, 29.8% ± 3.6%ID/g; trastuzumab-Mal-D-GEEEK-[125I]IB, 45.3% ± 5.3%ID/g) and was significantly higher for 125I at all time points. In general, normal tissue levels were lower for

  19. Agent engineering

    CERN Document Server

    Liu, Jiming; Zhong, Ning; Wang, Patrick S P

    2001-01-01

    Agent engineering concerns the development of autonomous computational or physical entities capable of perceiving, reasoning, adapting, learning, cooperating and delegating in a dynamic environment. It is one of the most promising areas of research and development in information technology, computer science and engineering. This book addresses some of the key issues in agent engineering: What is meant by "autonomous agents"? How can we build agents with autonomy? What are the desirable capabilities of agents with respect to surviving (they will not die) and living (they will furthermore enjoy

  20. Superparamagnetic iron oxide--loaded poly(lactic acid)-D-alpha-tocopherol polyethylene glycol 1000 succinate copolymer nanoparticles as MRI contrast agent.

    Science.gov (United States)

    Prashant, Chandrasekharan; Dipak, Maity; Yang, Chang-Tong; Chuang, Kai-Hsiang; Jun, Ding; Feng, Si-Shen

    2010-07-01

    We developed a strategy to formulate supraparamagnetic iron oxides (SPIOs) in nanoparticles (NPs) of biodegradable copolymer made up of poly(lactic acid) (PLA) and d-alpha-tocopherol polyethylene glycol 1000 succinate (TPGS) for medical imaging by magnetic resonance imaging (MRI) of high contrast and low side effects. The IOs-loaded PLA-TPGS NPs (IOs-PNPs) were prepared by the single emulsion method and the nanoprecipitation method. Effects of the process parameters such as the emulsifier concentration, IOs loading in the nanoparticles, and the solvent to non-solvent ratio on the IOs distribution within the polymeric matrix were investigated and the formulation was then optimized. The transmission electron microscopy (TEM) showed direct visual evidence for the well dispersed distribution of the IOs within the NPs. We further investigated the biocompatibility and cellular uptake of the IOs-PNPs in vitro with MCF-7 breast cancer cells and NIH-3T3 mouse fibroblast in close comparison with the commercial IOs imaging agent Resovist. MRI imaging was further carried out to investigate the biodistribution of the IOs formulated in the IOs-PNPs, especially in the liver to understand the liver clearance process, which was also made in close comparison with Resovist. We found that the PLA-TPGS NPs formulation at the clinically approved dose of 0.8 mg Fe/kg could be cleared within 24 h in comparison with several weeks for Resovist. Xenograft tumor model MRI confirmed the advantages of the IOs-PNPs formulation versus Resovist through the enhanced permeation and retention (EPR) effect of the tumor vasculature. PMID:20434210

  1. A Series of Oleanolic Acid Derivatives as Anti-Hepatitis B Virus Agents: Design, Synthesis, and in Vitro and in Vivo Biological Evaluation

    Directory of Open Access Journals (Sweden)

    Wenqiang Yan

    2016-03-01

    Full Text Available A series of oleanolic acid derivatives were synthesized by diverse reactions, including the introduction of conjugated alkadiene and epoxy ring moieties formed by means of photosensitized oxidation. Eosin Y was used as photosensitizer during this process. Next the cytotoxicity of the products was evaluated on HepG2.2.15 cells to determine the appropriate treatment concentration for the subsequent experiments. Most of the OA derivatives exhibited anti-HBV antigens secretion activity in HepG2.2.15 cells. Among the tested compounds, OA-4 (3.13 µg/mL showed significant activity against the secretion of HBsAg, HBeAg, and HBV DNA replication with inhibitory ratios of 90.52% ± 1.78%, 31.55% ± 3.65%, and 94.57% ± 3.11% after 6 days, respectively. Besides, OA-4 was further investigated in a duck model with DHBV infection. When OA-4 was administered at a dosage of 500 mg/kg, the results revealed a significant inhibitory effects of DHBV at 19.94% ± 2.87%, 28.80% ± 3.62% and 29.25% ± 2.65% at days 5, 10, and 3 after the cessation of OA-4 treatment, respectively. It’s worth noting that OA-4 is superior to lamivudine in the inhibition of rebound of viral replication rate. The structure–activity relationships of OA derivatives had been preliminary discussed, which should be useful to explore further novel anti-HBV agents.

  2. A Series of Oleanolic Acid Derivatives as Anti-Hepatitis B Virus Agents: Design, Synthesis, and in Vitro and in Vivo Biological Evaluation.

    Science.gov (United States)

    Yan, Wenqiang; Zhang, Chenze; Li, Bi; Xu, Xin; Liang, Miao; Gu, Shun; Chu, Fuhao; Xu, Bing; Ren, Jian; Wang, Penglong; Lei, Haimin

    2016-01-01

    A series of oleanolic acid derivatives were synthesized by diverse reactions, including the introduction of conjugated alkadiene and epoxy ring moieties formed by means of photosensitized oxidation. Eosin Y was used as photosensitizer during this process. Next the cytotoxicity of the products was evaluated on HepG2.2.15 cells to determine the appropriate treatment concentration for the subsequent experiments. Most of the OA derivatives exhibited anti-HBV antigens secretion activity in HepG2.2.15 cells. Among the tested compounds, OA-4 (3.13 µg/mL) showed significant activity against the secretion of HBsAg, HBeAg, and HBV DNA replication with inhibitory ratios of 90.52% ± 1.78%, 31.55% ± 3.65%, and 94.57% ± 3.11% after 6 days, respectively. Besides, OA-4 was further investigated in a duck model with DHBV infection. When OA-4 was administered at a dosage of 500 mg/kg, the results revealed a significant inhibitory effects of DHBV at 19.94% ± 2.87%, 28.80% ± 3.62% and 29.25% ± 2.65% at days 5, 10, and 3 after the cessation of OA-4 treatment, respectively. It's worth noting that OA-4 is superior to lamivudine in the inhibition of rebound of viral replication rate. The structure-activity relationships of OA derivatives had been preliminary discussed, which should be useful to explore further novel anti-HBV agents. PMID:27023498

  3. Hydroxycarboxylic acids and salts

    Energy Technology Data Exchange (ETDEWEB)

    Kiely, Donald E; Hash, Kirk R; Kramer-Presta, Kylie; Smith, Tyler N

    2015-02-24

    Compositions which inhibit corrosion and alter the physical properties of concrete (admixtures) are prepared from salt mixtures of hydroxycarboxylic acids, carboxylic acids, and nitric acid. The salt mixtures are prepared by neutralizing acid product mixtures from the oxidation of polyols using nitric acid and oxygen as the oxidizing agents. Nitric acid is removed from the hydroxycarboxylic acids by evaporation and diffusion dialysis.

  4. The effect of dual complexing agents of lactic and citric acids on the formation of sol-gel derived Ag–PbTiO{sub 3} percolative thin film

    Energy Technology Data Exchange (ETDEWEB)

    Su, Yanbo; Hu, Tao; Tang, Liwen; Weng, Wenjian; Han, Gaorong; Ma, Ning; Du, Piyi, E-mail: dupy@zju.edu.cn

    2014-05-02

    Controlling the formation of conductive particles to be nano-scale is important for achieving percolation effect in metal dispersed thin film composite to contribute extraordinary dielectric properties required for miniaturization of electronic devices. In this paper, lactic acid (LA) and citric acid (CA) were used as dual complexing agents to prepare a typical Ag nanoparticle dispersed PbTiO{sub 3} (PTO) composite thin film by using a sol-gel method. The phase structure of the thin film and the coordination effect between complexing agent and metallic ions were investigated. It revealed that LA coordinated with Ti{sup 4+} and Pb{sup 2+} and CA coordinated with Ag{sup +}. Lead was fixed inside the gel network by LA and restricted to evaporate during heat treatment thus the pyrochlore phase was prevented from forming in the thin film. Ag{sup +} was coordinated by CA and the diffusion and thus aggregation of silver during gelation and annealing process were weakened. Silver nanoparticles dispersed in the PTO matrix formed with dual complexing agents of LA and CA introduced during the preparation process. The composite thin film of perfect perovskite phase with silver nanoparticles embedded was obtained at the molar ratio of LA/lead = 0.5 and CA/lead = 0.5. The dielectric constant of the thin film with silver nanoparticles is 5 times higher than that without silver nanoparticles. - Highlights: • Ag nanoparticle–PbTiO{sub 3} percolative film with high dielectric property is prepared. • Evaporation of lead was prevented by coordinating Pb with lactic acid agent. • Dual complexing agents contribute block and pinning effects to form Ag nanoparticles.

  5. System a amino acid transport-targeted brain and systemic tumor PET imaging agents 2-amino-3-[18 F]fluoro-2-methylpropanoic acid and 3-[18 F]fluoro-2-methyl-2-(methylamino)propanoic acid

    International Nuclear Information System (INIS)

    Introduction: Amino acid based radiotracers target tumor cells through increased uptake by membrane-associated amino acid transport (AAT) systems. In the present study, four structurally related non-natural 18 F-labeled amino acids, (R)- and (S)-[18 F]FAMP 1 and (R)- and (S)-[18 F]MeFAMP 2 have been prepared and evaluated in vitro and in vivo for their potential utility in brain and systemic tumor imaging based upon primarily system A transport with positron emission tomography (PET). Methods: The transport of enantiomers of [18 F]FAMP 1 and [18 F]MeFAMP 2 was measured through in vitro uptake assays in human derived cancer cells including A549 (lung), DU145 (prostate), SKOV3 (ovary), MDA MB468 (breast) and U87 (brain) in the presence and absence of amino acid transporter inhibitors. The in vivo biodistribution of these tracers was evaluated using tumor mice xenografts at 15, 30, 60 and 120 min post injection. Results: All four tracers showed moderate to high levels of uptake (1–9%ID/5 × 105 cells) by the cancer cell lines tested in vitro. AAT cell inhibition assays demonstrated that (R)-[18 F]1 and (S)-[18 F]1 entered these tumor cells via mixed AATs, likely but not limited to system A and system L. In contrast, (R)-[18 F]2 and (S)-[18 F]2 showed high selectivity for system A AAT. Similar to the results of in vitro cell studies, the tumor uptake of all four tracers was good to high and persisted over the 2 hours time course of in vivo studies. The accumulation of these tracers was higher in tumor than most normal tissues including blood, brain, muscle, bone, heart, and lung, and the tracers with the highest in vitro selectivity for system A AAT generally demonstrated the best tumor imaging properties. Higher uptake of these tracers was observed in the pancreas, kidney and spleen compared to tumors. Conclusions: These preclinical studies demonstrate good imaging properties in a wide range of tumors for all four amino acids evaluated with (R)-[18 F]2 having the

  6. Radioactive diagnostic agent

    International Nuclear Information System (INIS)

    A dispersion of denatured aggregates of serum albumin to which tin is attached is prepared and lyophilized. A mixture of polycarboxylic acid and a disaccharide or monosaccharide is included in the dispersion in sufficient amount to reduce degradation during lyophilization and aging. The dispersion is suitable for radioactive labelling and use as a diagnostic agent

  7. 以有机酸钾盐为可燃剂的气溶胶灭火剂试验%Experimental study on aerosol fire extinguishing agent with organic acid potassium as combustible material

    Institute of Scientific and Technical Information of China (English)

    王鹏; 李玉

    2011-01-01

    用1 m密闭试验葙进行灭火性能试验,采用半分法得出两种以有机酸钾盐为主要可燃剂的气溶胶灭火剂的配方,并对比其灭火时间.在热气溶胶灭火剂中添加碳酸钾作为热耗散剂,以降低反应速度,减小火焰外喷.用兰利法进行试验,得出了两种灭火剂的99%概率灭火效能,在70~75 g/m之间.经测量,气溶胶灭火剂的燃烧产物是低毒的.气溶胶灭火剂在灭火时的不确定度很大,应以概率论的方法研究其灭火能力.%An airtight box with 1 m3 was used to test fire extinguishing performance; two kinds of aerosol fire extinguishing agents with organic acid potassium as combustible material were got by split- half method, and the fire- extinguishing time was compared. Potassium carbonate was added into aerosol fire extinguishing agents as heat dissipative agents to slow down the reaction and reduce the flame. Langlie method was used in experiments, the 99% application density of these twa extinguishing agents were got, between 70~75 g/m3. At last, the toxicity of combustion product of these two aerosol fire extinguishing agents was tested to be low. The application of probability theory in the study of fire extinguishing performance of aerosol fire extinguishing agent is necessary because of the uncertainty of putting out fire by aerosol fire extinguishing agents.

  8. Successful treatment of pediatric IgG4 related systemic disease with mycophenolate mofetil: case report and a review of the pediatric autoimmune pancreatitis literature

    Directory of Open Access Journals (Sweden)

    Cron Randy Q

    2011-01-01

    Full Text Available Abstract Autoimmune pancreatitis is frequently associated with elevated serum and tissue IgG4 levels in the adult population, but there are few reports of pediatric autoimmune pancreatitis, and even fewer reports of IgG4 related systemic disease in a pediatric population. The standard of care treatment in adults is systemic corticosteroids with resolution of symptoms in most cases; however, multiple courses of corticosteroids are occasionally required and some patients require long term corticosteroids. In these instances, steroid sparing disease modify treatments are in demand. We describe a 13-year-old girl with IgG4 related systemic disease who presented with chronic recurrent autoimmune pancreatitis resulting in surgical intervention for obstructive hyperbilirubinemia and chronic corticosteroid treatment. In addition, she developed fibrosing medianstinitis as part of her IgG4 related systemic disease. She was eventually successfully treated with mycophenolate mofetil allowing for discontinuation of corticosteroids. This is the first reported use of mycophenolate mofetil for IgG4 related pancreatitis. Although autoimmune pancreatitis as part of IgG4 related systemic disease is rarely reported in pediatrics, autoimmune pancreatitis is also characterized as idiopathic fibrosing pancreatitis. All pediatric autoimmune pancreatitis cases reported in the world medical literature were identified via a PUBMED search and are reviewed herein. Twelve reports of pediatric autoimmune pancreatitis were identified, most of which were treated with corticosteroids or surgical approaches. Most case reports failed to report IgG4 levels, so it remains unclear how commonly IgG4 related autoimmune pancreatitis occurs during childhood. Increased evaluation of IgG4 levels in patients with autoimmune pancreatitis may shed further light on the association of IgG4 with pancreatitis and the underlying pathophysiology.

  9. Cobalt bis(dicarbollide) ions with covalently bonded CMPO groups as selective extraction agents for lanthanide and actinide cations from highly acidic nuclear waste solutions

    International Nuclear Information System (INIS)

    A new series of boron substituted cobalt bis(dicarbollide)(1-) ion (1) derivatives of the general formula [(8-CMPO-(CH2-CH2O)2-1,2-C2B9H10)(1',2'-C2B9H11)-3,3'-Co]- (CMPO = Ph2P(O)-CH2C(O)NR, R = C4H9 (3b), -C12H25 (4b), -CH2-C6H5 (5b)) was prepared by ring cleavage of the 8-dioxane-cobalt bis(dicarbollide) (2) bi-polar compound by the respective primary amines and by subsequent reaction of the resulting amino derivatives (3a-5a) with the nitrophenyl ester of diphenyl-phosphoryl-acetic acid. The compounds were synthesized with the aim to develop a new class of more efficient extraction agents for liquid/liquid extraction of polyvalent cations, i.e. lanthanides and actinides, from high-level activity nuclear waste. All compounds were characterized by a combination of 11B NMR, 1H high field NMR, Mass Spectrometry with Electro-spray and MALDI TOF ionisation, HPLC and other techniques. The molecular structure of the supramolecular Ln3+ complex of the anion 5b was determined by single crystal X-ray diffraction analysis. Crystallographic results proved that the Ln(m) atom is bonded to three functionalized cobalt bis(dicarbollide) anions in a charge compensated complex. The cation is tightly coordinated by six oxygen atoms of the CMPO terminal groups (two of each ligand) and by three water molecules completing the metal coordination number to 9. Atoms occupying the primary coordination sphere form a tri-capped trigonal prismatic arrangement. Very high liquid-liquid extraction efficiency of all anionic species was observed. Moreover, less polar toluene can be applied as an auxiliary solvent replacing the less environmentally friendly nitro- and chlorinated solvents used in the current dicarbollide liquid-liquid extraction process. The extraction coefficients are sufficiently high for possible technological applications. (authors)

  10. The Antimicrobial Agent Fusidic Acid Inhibits Organic Anion Transporting Polypeptide-Mediated Hepatic Clearance and May Potentiate Statin-Induced Myopathy.

    Science.gov (United States)

    Eng, Heather; Scialis, Renato J; Rotter, Charles J; Lin, Jian; Lazzaro, Sarah; Varma, Manthena V; Di, Li; Feng, Bo; West, Michael; Kalgutkar, Amit S

    2016-05-01

    Chronic treatment of methicillin-resistantStaphylococcus aureusstrains with the bacteriostatic agent fusidic acid (FA) is frequently associated with myopathy including rhabdomyolysis upon coadministration with statins. Because adverse effects with statins are usually the result of drug-drug interactions, we evaluated the inhibitory effects of FA against human CYP3A4 and clinically relevant drug transporters such as organic anion transporting polypeptides OATP1B1 and OATP1B3, multidrug resistant protein 1, and breast cancer resistance protein, which are involved in the oral absorption and/or systemic clearance of statins including atorvastatin, rosuvastatin, and simvastatin. FA was a weak reversible (IC50= 295 ± 1.0μM) and time-dependent (KI= 216 ± 41μM andkinact= 0.0179 ± 0.001 min(-1)) inhibitor of CYP3A4-catalyzed midazolam-1'-hydroxylase activity in human liver microsomes. FA demonstrated inhibition of multidrug resistant protein 1-mediated digoxin transport with an IC50value of 157 ± 1.0μM and was devoid of breast cancer resistance protein inhibition (IC50> 500μM). In contrast, FA showed potent inhibition of OATP1B1- and OATP1B3-specific rosuvastatin transport with IC50values of 1.59μM and 2.47μM, respectively. Furthermore, coadministration of oral rosuvastatin and FA to rats led to an approximately 19.3-fold and 24.6-fold increase in the rosuvastatin maximum plasma concentration and area under the plasma concentration-time curve, respectively, which could be potentially mediated through inhibitory effects of FA on rat Oatp1a4 (IC50= 2.26μM) and Oatp1b2 (IC50= 4.38μM) transporters, which are responsible for rosuvastatin uptake in rat liver. The potent inhibition of human OATP1B1/OATP1B3 by FA could attenuate hepatic uptake of statins, resulting in increased blood and tissue concentrations, potentially manifesting in musculoskeletal toxicity. PMID:26888941

  11. Safety test of a supplement, 5-aminolevulinic acid phosphate with sodium ferrous citrate, in diabetic patients treated with oral hypoglycemic agents

    Directory of Open Access Journals (Sweden)

    Naohide Yamashita

    2014-09-01

    Full Text Available Objective: This study aimed to examine the safety of 5-aminolevulinic acid phosphate (5-ALA with sodium ferrous citrate (SFC in diabetic patients treated with one or more oral hypoglycemic agents (OHAs. Background: Recent intervention studies performed in the USA and Japan have shown that a nutritional supplement of 5-ALA with SFC efficiently reduced blood glucose levels in pre-diabetic population without any adverse events. Thus, it was anticipated that 5-ALA with SFC may potentially be taken as a beneficial supplement by diabetic patients who were being treated with OHA therapy. Nevertheless, it is important to examine its safety and efficacy in diabetic population. Methods: This study was a prospective single-blinded, randomized, placebo-controlled and parallel-group comparison study. Medically treated diabetic patients between the ages of 30 and 75 were recruited from the Tokyo metropolitan area of Japan and 45 subjects were selected after screening. These subjects were randomly assigned to three groups: daily intake of 15mg 5-ALA, 50mg 5-ALA, and a placebo (n=15, respectively. The supplement or placebo was administered for 12 weeks followed by a four week washout period. The primary endpoint was safety and occurrence of hypoglycemic attack, while the secondary endpoint was changes of fasting blood glucose (FBG and hemoglobin A1c (HbA1c. Results: Adverse events related to 5-ALA with SFC were not observed in all the groups. Abnormalities in blood and urine tests were not observed either. Significant decrease in FBG was not detected in all the groups. However, there was a small but significant decrease in HbA1c at 4 and 8 week in the 15 mg 5-ALA group. Significant decrease in HbA1c was not observed in the 50 mg 5-ALA group, although a tendency to decrease after 4 weeks was apparent. Conclusion: 5-ALA with SFC is a safe and potentially beneficial supplement if taken by diabetic patients treated with OHAs.

  12. Antibiotic Agents

    Science.gov (United States)

    ... either as public health or as non-public health antimicrobial agents. What is the difference between bacteriostats, sanitizers, disinfectants ... bacteria, however, there is considerable controversy surrounding their health benefits. The ... producing agents (Table of Antibacterials) have been used for many ...

  13. Evaluation of copper speciation in model solutions of humic acid by mini-columns packed with Chelex-100 and new chelating agents: Application to speciation of selected heavy metals in environmental water samples

    International Nuclear Information System (INIS)

    A solid-phase extraction procedure using mini-columns packed with Chelex-100 and two new chelating agents based on poly(vinyl chloride) functionalized with 3-ferrocenyl-3-hydroxydithioacrylic acid and N,N'-[1,1'-dithiobis(ethylene)]-bis(salicylideneimine) (H2sales) loaded on microcrystalline naphthalene, is reported. The columns were used to separate labile copper fractions in model solutions and in real samples with subsequent determination using electrothermal atomic absorption spectrometry (ETAAS). Various model solutions containing 20 μg L-1 of Cu2+ and 0.0, 0.2, 2.0 and 20.0 mg L-1 of humic acid, respectively, and buffered to pH 6.0, 7.0 and 8.0 were considered. Results showed a decrease in labile copper fraction with increase in humic acid concentration. Application of the procedure to speciation of Cu, Ni, Zn and Pb in various environmental water samples yielded labile fractions in the range of 1.67-55.75% against a total dissolved fraction of 44.08-69.77%. Comparison of the three chelating agents showed that H2sales had a weaker metal chelating strength than Chelex-100, but PVC-FSSH had comparable chelating strength to Chelex-100.

  14. Chelating agents related to ethylenediamine bis(2-hydroxyphenyl)acetic acid (EDDHA): synthesis, characterization, and equilibrium studies of the free ligands and their Mg2+, Ca2+, Cu2+, and Fe3+ chelates.

    Science.gov (United States)

    Yunta, Felipe; García-Marco, Sonia; Lucena, Juan J; Gómez-Gallego, Mar; Alcázar, Roberto; Sierra, Miguel A

    2003-08-25

    Iron chelates such as ethylenediamine-N,N'-bis(2-hydroxyphenyl)acetic acid (EDDHA) and their analogues are the most efficient soil fertilizers to treat iron chlorosis in plants growing in calcareous soils. EDDHA, EDDH4MA (ethylenediamine-N,N'-bis(2-hydroxy-4-methylphenyl)acetic acid), and EDDCHA (ethylenediamine-N,N'-bis(2-hydroxy-5-carboxyphenyl)acetic acid) are allowed by the European directive, but also EDDHSA (ethylenediamine-N,N'-bis(2-hydroxy-5-sulfonylphenyl)acetic acid) and EDDH5MA (ethylenediamine-N,N'-bis(2-hydroxy-5-methylphenyl)acetic acid) are present in several commercial iron chelates. In this study, these chelating agents as well as p,p-EDDHA (ethylenediamine-N,N'-bis(4-hydroxyphenyl)acetic acid) and EDDMtxA (ethylenediamine-N,N'-bis(2-metoxyphenyl)acetic acid) have been obtained following a new synthetic pathway. Their chemical behavior has been studied to predict the effect of the substituents in the benzene ring on their efficacy as iron fertilizers for soils above pH 7. The purity of the chelating agents has been determined using a novel methodology through spectrophotometric titration at 480 nm with Fe(3+) as titrant to evaluate the inorganic impurities. The protonation constants were determined by both spectrophotometric and potentiometric methods, and Ca(2+) and Mg(2+) stability constants were determined from potentiometric titrations. To establish the Fe(3+) and Cu(2+) stability constants, a new spectrophotometric method has been developed, and the results were compared with those reported in the literature for EDDHA and EDDHMA and their meso- and rac-isomers. pM values have been also determined to provide a comparable basis to establish the relative chelating ability of these ligands. The purity obtained for the ligands is higher than 87% in all cases and is comparable with that obtained by (1)H NMR. No significant differences have been found among ligands when their protonation and stability constants were compared. As expected, no Fe(3

  15. 新型硫化物助剂强化浸出酸浸渣中铁的研究%Study on Intensified Leaching of Ferric Iron from Acid-leach Residues Using Sulfide as a Novel Leaching Agent

    Institute of Scientific and Technical Information of China (English)

    金程; 赵颖华; 李登新

    2011-01-01

    采用硫化物作助剂强化溶浸酸浸渣中的氧化铁.分别进行了助浸剂用量、硫酸用量、时间、温度、液固比等条件试验,考察其对酸溶效果的影响,结果表明:当助剂与渣质量比为0.69:1,硫酸过剩系数为1.4,起始液固比为2:1,搅拌速度为1 300 r/min时,在95℃下反应2h,铁的浸取率可以达到89.2%,助剂中锌的浸出率为90.2%,尾渣易于进一步提金.与现行技术条件相比,硫酸用量大大减少,工艺简单,能耗低.%Taking sulfide as a leaching agent, tests were conducted on the intensified-leaching of iron oxide from acid-leach residue. Influence of different factors, such as consumption of leaching agent, dosage of sulfuric acid, leaching time and temperature, as well as liquid-solid ratio, on the leaching effect was investigated. Results show that iron leaching rate reaches 89.2% and the leach rate of zinc from leaching agent is 90.2% under the following conditions of the initial liquid/solid ratio being 1'-1, the mass ratio of leaching agent to residue being 0. 69: 1, excess coefficient of sulfuric acid being 1.4, with a stirring rate at 1 300 r/min and reaction at the temperature of 95 X. For 2 h. The tailings obtained can also be used for further gold-extraction. This process is simple with low energy consumption compared with the existing technology, and sulfuric acid consumption is greatly reduced.

  16. Preparation and properties of N-Phenylbutyrohydroxamic acid and N-p-Chlorophenylbutyrohydroxamic acid and their uses as extracting agents for Chromium (VI), Molybdenum (VI), Titanium (IV) and Uranium (VI)

    International Nuclear Information System (INIS)

    Two lignads, N-phenylbutyrohydroxamic acid (1), N-p-chlorophenylbutyryl chloride with β phenyl-hydroylamine and N-p-chlorophenylhydroxylamine, respectively. The acids prepared were identified and characterised through their reactions with Vanadiun (V) and iron (III), their melting points, infra-red spectra and nitrogen content. The extractive properties of these acids towards the metals Cr (VI), Mo (VI), Ti (IV) and U (VI) were examined at different PH values. The percentage of maximum extraction with the two acids was found to be as follows : for Cr (VI) at PH 1, (100%) for both acids, Mo (VI) at PH 2 (33.34%) with acid (I) and (16.67%) with acid (II) and U (VI) at PH 6 (72%) with acid (I) and (76%) with acid (II). The metal: Ligand complexes ratios were determined by using the continuous variation method, the ratio of the two ligands with four metals was found to be 1:2. Finally the suitability of the two acids for spectrophotometric determination of four metals was examined.(Author)

  17. Reducing-Agent-Free Instant Synthesis of Carbon-Supported Pd Catalysts in a Green Leidenfrost Droplet Reactor and Catalytic Activity in Formic Acid Dehydrogenation

    OpenAIRE

    Dong-Wook Lee; Min-Ho Jin; Young-Joo Lee; Ju-Hyoung Park; Chun-Boo Lee; Jong-Soo Park

    2016-01-01

    The development of green synthesis methods for supported noble metal catalysts remains important challenges to improve their sustainability. Here we first synthesized carbon-supported Pd catalysts in a green Leidenfrost droplet reactor without reducing agents, high-temperature calcination and reduction procedures. When the aqueous solution containing Pd nitrate precursor, carbon support, and water is dripped on a hot plate, vapor layer is formed between a solution droplet and hot surface, whi...

  18. Effects of alumina air-abrasion and acidic priming agents on bonding between SUS XM27 steel and auto-polymerizing acrylic resin.

    Science.gov (United States)

    Ishikawa, Yumi; Ohashi, Norihisa; Koizumi, Hiroyasu; Tanoue, Naomi; Nishiyama, Norihiro; Matsumura, Hideo

    2007-09-01

    The purpose of this study was to evaluate the effects of functional monomers contained in the primers, as well as alumina particle abrasion on bonding between stainless steel and acrylic resin. SUS XM27 steel was primed with one of the following materials; Alloy Primer, Estenia Opaque Primer, M. L. Primer, and Super-Bond Liquid. Steel disks were either ground flat or alumina-blasted, primed with one of the four agents, and bonded with an acrylic resin (Unifast Trad). Bond strength was determined both before and after thermocycling (2,000 or 20,000 cycles). Among the four priming agents, the Alloy Primer and Estenia Opaque Primer, both of which contain 10-methacryloyloxydecyl dihydrogen phosphate (MDP), exhibited better bonding performance than the others. Alumina air-borne particle abrasion considerably improved the durability of bonding between the steel and the resin material. It can be concluded that alumina blasting followed by priming with an MDP agent is recommended for bonding the resin and SUS XM27 steel. PMID:17928724

  19. Agent, autonomous

    OpenAIRE

    Luciani, Annie

    2007-01-01

    The expression autonomous agents, widely used in virtual reality, computer graphics, artificial intelligence and artificial life, corresponds to the simulation of autonomous creatures, virtual (i.e. totally computed by a program), or embodied in a physical envelope, as done in autonomous robots.

  20. TWO-YEAR OBSERVATION OF A RANDOMIZED TRIAL ON TACROLIMUS-BASED THERAPY WITH WITHDRAWAL OF STEROIDS OR MYCOPHENOLATE MOFETIL AFTER RENAL TRANSPLANTATION

    Institute of Scientific and Technical Information of China (English)

    Qing-guo Zhu; Ya-kun Zhao; Wei Liu; Hui Luo; Yu Qiu; Zhi-zhong Gao

    2008-01-01

    Objective To evaluate the safety and feasibility of steroid or mycophenolate mofetil (MMF) withdrawal from tacrolimus-based immunosuppressant regimen in renal allograft recipients.Methods A cohort of 45 patients following cadaveric renal allograft transplantation were randomly divided into 3 groups based on the regimen of combination of taerolimus,steroid,and MMF:triple therapy group,steroid withdrawal group,and MMF withdrawal group.During 2 years,survival of patients and aUografls,clinical acute rejection,adverse events,hepatic and renal allograft function,and blood lipids were monitored to evaluate the safety and feasibility of steroid or MMF withdrawal after renal transplantation.Results During two-year observation,steroid or MMF was successfully withdrawn from immunosuppressant regimen based on tacrolimus without any clinical acute rejection.Patient and graft survival rates were 100% and all the renal allografts kept excellent function.Some adverse events occurred and there were no significant differences among groups.Conclusion Withdrawal of steroid or MMF in low-immunological-risk renal allografts treated with taerolimus-based immunosuppressant regimen can be achieved with no increased risk of acute rejection.

  1. Design, Synthesis and Biological Evaluation of Hydroxamic Acid Derivatives as Potential High Density Lipoprotein (HDL) Receptor CLA-1 Up-Regulating Agents

    OpenAIRE

    Yu Du; Yanbin Wu; Bin Hong; Yuan Yang; Xiaojian Jia; Li Wang; Xiaofang Chen

    2011-01-01

    Trichostatin A (TSA) and suberoylanilide hydroxamic acid (SAHA) were reported in our recent publication as novel human high density lipoprotein (HDL) receptor CD36 and Lysosomal integral membrane protein-II Analogous-1 (CLA-1) up-regulators. As part of a broader effort to more fully explore the structure-activity relationships (SAR) of CLA-1 up-regulators, we synthesized a series of hydroxamic acid derivatives and evaluated their CLA-1 up-regulating activities in HepG2 cells. Some compounds e...

  2. Distinctive behaviour of 99Tcsup(m)(V) dimercaptosuccinic acid as a tumour-seeking agent: Usefulness for the diagnosis of head and neck tumours, medullary thyroid cancers and soft-tissue tumours

    International Nuclear Information System (INIS)

    Considering the ideal nuclear properties of 99Tcsup(m), a new 99Tcsup(m)-labelled radiopharmaceutical has been developed for tumour imaging. Dimercaptosuccinic acid (DMS) has been chosen as ligand and SnCl2 as reducing agent. The highest uptake by tumour cells was obtained when the 99Tcsup(m) complex was in oxidation state V. This newly designed tumour-seeking agent, 99Tcsup(m)(V) DMS, showed a distribution behaviour different from that of the well-known renal scanning agent, 99Tcsup(m)(III) DMS, which was considered to be in oxidation state III. Basic studies, carried out in vitro and in vivo with Ehrlich tumour cells of tumour-bearing mice, clearly substantiated the great potential of 99Tcsup(m)(V) DMS for clinical use. Therefore, 193 untreated patients with a histologically proven diagnosis of cancer were scanned for 99Tcsup(m)(V) DMS uptake. This radiopharmaceutical was particularly useful for scanning of head and neck squamous cell carcinomas, medullary thyroid cancers and soft-tissue tumours. Also the superior physical properties of 99Tcsup(m), which gave better images within two hours after injection, together with the easy method and the low cost, justify its use in preference to 67Ga. The great importance of the 99Tcsup(m) oxidation state with regard to its biological behaviour, and the different tumour uptake mechanisms of 99Tcsup(m)(V) DMS and 67Ga or 201Tl could be shown. The data collected provide a good basis for the clinical applicability of 99Tcsup(m)(V) DMS as a tumour-imaging agent. (author)

  3. Gadolinium(III) complexes of mono- and diethyl esters of monophosphonic acid analogue of DOTA as potential MRI contrast agents: solution structures and relaxometric studies

    OpenAIRE

    Lebduskova, Petra; Hermann, Petr; Helm, Lothar; Toth, Eva; Kotek, Jan; Binnemans, Koen; Rudovsky, Jakub; Lukes, Ivan; Merbach, Andre E

    2007-01-01

    Two new macrocyclic DOTA-like chelates containing one phosphonate pendant arm were synthesised as potential contrast agents for MRI ( magnetic resonance imaging). The chelates bind to the lanthanide(III) in an octadentate manner, via four nitrogen atoms, three carboxylate and one phosphonate oxygen atoms. Solution structures of [Ln(do3apO(Et2))(H2O)] and [Ln(do3ap(OEt))(H2O)](-) were studied using P-31 and H-1 NMR spectroscopy and SAP (square-antiprismatic)/TSAP ( twisted square-antiprismatic...

  4. The Increased Promotion in Cobalt-Molybdenum Hydrodesulfurization Catalysts Supported on Alumina, Activated Carbon and Zirkonia by the Chelating Agent Nitrilotriacetic Acid

    OpenAIRE

    Kaluža, Luděk

    2013-01-01

    The most active CoMo/Al2O3, C and ZrO2 catalysts in benzothiophene HDS were prepared by the impregnation of the support from the solution made by dissolution of MoO3, CoCO3 and nitrilotriacetic acid in water followed by sulfidation without previous calcination.

  5. Development of HPLC and UV spectrophotometric methods for the determination of ascorbic acid using hydroxypropyl-β-cyclodextrin and triethanolamine as photostabilizing agents

    International Nuclear Information System (INIS)

    In this study, the effect of complex formation with triethanolamine (TEA) alone and in combination with hydroxypropyl-β-cyclodextrin (HP-β-CD) on the photostability of ascorbic acid was evaluated for exposure to artificial and diffuse daylight. The first-order rate constants for the photodegradation reactions were determined. The data obtained showed that these complexes strongly reduced the photodegradation process with an 11- and 35-fold increase in the photostability of ascorbic acid, depending of the ligand concentration and the irradiation source. The multicomponent complex gave a significantly better stabilization for exposure to light than TEA alone. Due to the fact that the complexation extended the exposure of ascorbic acid to light (without molecular changes), UV spectrophotometric and reversed phase high performance liquid chromatographic (HPLC) methods were developed for the quantitative determination of the vitamin in pure form and in pharmaceutical preparations. These methods were statistically validated, all the validation parameters were found to be within the acceptance range. These results demonstrate that the proposed methods are suitable for the quality control of ascorbic acid, providing simple, rapid, precise, accurate and convenient approaches for routine analysis of bulk drug and pharmaceutical formulations.

  6. Metal based pharmacologically active agents: Synthesis, structural characterization, molecular modeling, CT-DNA binding studies and in vitro antimicrobial screening of iron(II) bromosalicylidene amino acid chelates

    Science.gov (United States)

    Abdel-Rahman, Laila H.; El-Khatib, Rafat M.; Nassr, Lobna A. E.; Abu-Dief, Ahmed M.; Ismael, Mohamed; Seleem, Amin Abdou

    2014-01-01

    In recent years, great interest has been focused on Fe(II) Schiff base amino acid complexes as cytotoxic and antitumor drugs. Thus a series of new iron(II) complexes based on Schiff bases amino acids ligands have been designed and synthesized from condensation of 5-bromosalicylaldehyde (bs) and α-amino acids (L-alanine (ala), L-phenylalanine (phala), L-aspartic acid (aspa), L-histidine (his) and L-arginine (arg)). The structure of the investigated iron(II) complexes was elucidated using elemental analyses, infrared, ultraviolet-visible, thermogravimetric analysis, as well as conductivity and magnetic susceptibility measurements. Moreover, the stoichiometry and the stability constants of the prepared complexes have been determined spectrophotometrically. The results suggest that 5-bromosalicylaldehyde amino acid Schiff bases (bs:aa) behave as dibasic tridentate ONO ligands and coordinate to Fe(II) in octahedral geometry according to the general formula [Fe(bs:aa)2]ṡnH2O. The conductivity values between 37 and 64 ohm-1 mol-1 cm2 in ethanol imply the presence of nonelectrolyte species. The structure of the complexes was validated using quantum mechanics calculations based on accurate DFT methods. Geometry optimization of the Fe-Schiff base amino acid complexes showed that all complexes had octahedral coordination. In addition, the interaction of these complexes with (CT-DNA) was investigated at pH = 7.2, by using UV-vis absorption, viscosity and agarose gel electrophoresis measurements. Results indicated that the investigated complexes strongly bind to calf thymus DNA via intercalative mode and showed a different DNA binding according to the sequence: bsari > bshi > bsali > bsasi > bsphali. Moreover, the prepared compounds are screened for their in vitro antibacterial and antifungal activity against three types of bacteria, Escherichia coli, Pseudomonas aeruginosa and Bacillus cereus and three types of anti fungal cultures, Penicillium purpurogenium, Aspergillus

  7. 腐植酸钾/丙烯酸型保水剂的合成及性能研究%Synthesis and performance of potassium humate/acrylic acid water-retaining agent

    Institute of Scientific and Technical Information of China (English)

    魏友华; 顾铭茜; 季燕; 陈洪龄

    2013-01-01

    以腐植酸钾(KHA)与丙烯酸(AA)为原料,N,N-亚甲基双丙烯酰胺为交联剂,过K2SO4为引发剂,进行水溶液聚合,制备得到腐植酸钾/丙烯酸高吸水性保水树脂.研究了反应物比例、反应温度、交联剂、引发剂用量、中和度等因素对产物性能的影响.考察了产物的热稳定性、保水性能、耐电解质和重复使用性能.结果表明,树脂最大吸水率为609g·g-1,耐盐性良好,50℃环境温度下9h保水树脂仍有94.2%的保水率.%Potassium humate/acrylic acid water retention resin was prepared from potassium humate and acrylic acid by aqueous polymerization with the crosslinking agent of N, N-methylene-bis-acrylamide and the initiator of potassium persulfate. The effect of reactant ratio, reaction temperature, the amount of cross-linking agent and initiator, and the neutralization degree were investigated. In addition, thermal stability, water retention and reuse ability of the products were studied. Results show that the maximum water absorption ability of potassium humate/acrylic acid superabsorbent resin was 609g·g-1 for distilled water. At the environment temperature 50℃, the water retention resin still have 94.2% of the water retention rate after 9 hour.

  8. 核酸交联剂在食源致病菌活菌检测中应用的研究进展%Application of nucleic acid cross-linking agent on detecting viable foodborne pathogens

    Institute of Scientific and Technical Information of China (English)

    黄楚楚; 张志鸿; 余双; 孙马钰; 魏华; 许恒毅

    2015-01-01

    近年来,由食源致病菌引起的食品安全问题越来越受到人们的重视,如何快速准确检测食品中是否存在食源致病菌是食品安全研究的热点问题。基于PCR检测食源致病菌的方法因快速且特异性强而被广泛应用,然而普通的PCR检测方法难以消除死菌残留DNA导致的假阳性结果,因而无法对致病菌进行准确检测。核酸交联剂是一种含有两个或两个以上烷基化官能团的烷基化试剂,目前,在食源致病菌检测中应用的核酸交联剂主要为EMA和PMA。核酸交联剂通过一定方式的诱导可选择性的透过死菌的细胞膜并与DNA产生共价交联,从而强有力的抑制死菌DNA的PCR扩增,达到鉴别死菌和活菌的效果。本文就核酸交联剂在食源致病菌活菌检测中应用的研究进展进行了综述,以期能为相关研究者开发食源致病菌活菌检测方法提供参考。%In recent years, food safety issues cause more and more people's attention by foodborne pathogens, and how to quickly and accurately detect the foodborne pathogens in food is a hot issue in food safety research. The methods based on PCR to detect foodborne pathogenic bacteria are widely used for its rapid and strong specificity, however, it is difficult to eliminate false positive results for regular PCR due to the interference of DNA from dead bacteria, and thus it is inability for accurate detection of viable bacteria. Nucleic acid cross-linking agent is a kind of alkylating agent containing two or more than two alkylation functional groups. At present, ethidium bromide monoazide (EMA) and propidium monoazide (PMA) are the most widely used nucleic acid cross-linking agent in the detection of viable foodborne pathogens. The nucleic acid cross-linking agent could selectively penetrate through dead bacteria cell membranes and covalent cross-link their DNA, thus eliminate false signal from the PCR amplification of dead bacteria. This

  9. Application of nucleic acid cross-linking agent on detecting viable foodborne pathogens%核酸交联剂在食源致病菌活菌检测中应用的研究进展

    Institute of Scientific and Technical Information of China (English)

    黄楚楚; 张志鸿; 余双; 孙马钰; 魏华; 许恒毅

    2015-01-01

    In recent years, food safety issues cause more and more people's attention by foodborne pathogens, and how to quickly and accurately detect the foodborne pathogens in food is a hot issue in food safety research. The methods based on PCR to detect foodborne pathogenic bacteria are widely used for its rapid and strong specificity, however, it is difficult to eliminate false positive results for regular PCR due to the interference of DNA from dead bacteria, and thus it is inability for accurate detection of viable bacteria. Nucleic acid cross-linking agent is a kind of alkylating agent containing two or more than two alkylation functional groups. At present, ethidium bromide monoazide (EMA) and propidium monoazide (PMA) are the most widely used nucleic acid cross-linking agent in the detection of viable foodborne pathogens. The nucleic acid cross-linking agent could selectively penetrate through dead bacteria cell membranes and covalent cross-link their DNA, thus eliminate false signal from the PCR amplification of dead bacteria. This paper reviewed the application of nucleic acid cross-linking agent in the detection of viable foodborne pathogens, with an aim to provide references for researchers to develop viable pathogen detection methods.%近年来,由食源致病菌引起的食品安全问题越来越受到人们的重视,如何快速准确检测食品中是否存在食源致病菌是食品安全研究的热点问题。基于PCR检测食源致病菌的方法因快速且特异性强而被广泛应用,然而普通的PCR检测方法难以消除死菌残留DNA导致的假阳性结果,因而无法对致病菌进行准确检测。核酸交联剂是一种含有两个或两个以上烷基化官能团的烷基化试剂,目前,在食源致病菌检测中应用的核酸交联剂主要为EMA和PMA。核酸交联剂通过一定方式的诱导可选择性的透过死菌的细胞膜并与DNA产生共价交联,从而强有力的抑制死菌DNA的PCR扩

  10. A single-step synthesis of gold nanochains using an amino acid as a capping agent and characterization of their optical properties

    International Nuclear Information System (INIS)

    We demonstrated a simple single-step synthesis of gold nanochains by reducing aqueous chloroaurate ions (AuCl4-) with sodiumborohydride (NaBH4) in the presence of an amino acid (glutamic acid and histidine) as a stabilizer. The structure and optical properties of gold nanochains and nanowires were characterized by transmission electron microscopy, UV-visible spectroscopy, infrared spectroscopy and femtosecond z-scan measurements. The results suggested that the gold nanochains and nanowires were formed via the nanospheres fusing into one another by an oriented attachment mechanism through dipole-dipole interactions. The z-scan measurements on Au nanowires showed a transition from saturable absorption to reverse saturable absorption as the pump intensity increased

  11. Synthesis of carbon-14 labelled CD 271 (6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid): a potential new agent for dermatology

    International Nuclear Information System (INIS)

    6-[3-(1-Adamantyl)-4-methoxyphenyl]-2-naphthoic acid, a promising new compound for the treatment of disorders of keratinization, has been synthesized in [14C]-labelled form from barium[14C]-carbonate via labelled benzene. Benzene-[U-14C] was converted to 4-bromo-methoxybenzene-[phenyl-U-14C] in six steps. Introduction of the adamantyl ring was carried out using 1-acetoxyadamantane under acid catalysis. 2-(1-Adamantyl)-4-bromo-methoxybenzene-[phenyl-U-14C] was converted to a zincate and coupled with methyl 6-bromo-2-naphthoate using a nickel catalyst. The product of the aryl coupling reaction was then saponified to give 6-[3-(1-adamantyl)-4-methoxyphenyl-[phenyl-U-14C

  12. Synthesis, characterization and biological evaluation of N-ferrocenylmethyl amino acid benzene carboxamide derivatives and N-ferrocenyl benzoyl amino alkane derivatives as anti-cancer agents.

    OpenAIRE

    Butler, William E.

    2012-01-01

    The aim of this research was to explore the structure-activity relationship (SAR) of ferrocenyl-bioconjugates. A series of N-(ferrocenylmethylamino acid)-fluorinated-benzene carboxamide derivatives and a series of N-(ferrocenyl)-benzoyl-aminoalkane derivatives have been synthesised, structurally characterised and biologically evaluated for their anti-proliferative activity on various cancer cell lines, principally, the (estrogen receptor positive) MCF-7 breast cancer cell line. The anti-c...

  13. Effects of Organic Acids and Salts on the Development of Penicillium italicum: The Causal Agent of Citrus Blue Mold

    OpenAIRE

    Boudyach El Hassane; Serghini Mohammed Amine; Boubaker Hassan; Talibi Idriss; Askarne Latifa; Ait Ben Aoumar Abdellah

    2011-01-01

    Control of Citrus blue mold, caused by Penicillium italicum, has been accomplished by postharvest application of synthetic fungicides. However, the development of resistant fungal strains and increasing public concern over food safety and the environment are driving a search for alternative disease control strategies. In vitro trials were conducted to evaluate the effect of several organic acid and salt compounds on mycelial growth, sporulation, spore germination and germ tube elongation of P...

  14. Versatile Enzyme Expression and Characterization System for Aspergillus nidulans, with the Penicillium brevicompactum Polyketide Synthase Gene from the Mycophenolic Acid Gene Cluster as a Test Case

    DEFF Research Database (Denmark)

    Hansen, Bjarne Gram; Salomonsen, Bo; Nielsen, Morten Thrane;

    2011-01-01

    Assigning functions to newly discovered genes constitutes one of the major challenges en route to fully exploiting the data becoming available from the genome sequencing initiatives. Heterologous expression in an appropriate host is central in functional genomics studies. In this context, filamen...

  15. [On the chemistry of etofenamate, a novel anti-inflammatory agent from the series of N-arylanthranilic acid derivatives (author's transl)].

    Science.gov (United States)

    Boltze, K H; Kreisfeld, H

    1977-01-01

    Etofenamate is 2-(2-hydroxyethoxy)ethyl-N-(a,a,a,-trifluorom-tolyl)anthranilate and has been selected as an antiphlogistic agent for percutaneous therapy. Its characteristic alcohol-ether-ester structure brings about an increase in lipophilia and in its ability to penetrate through the intact skin. Furthermore, its oily consistency renders it ideal for pharmaceutical formulation in gels. The physico-chemical material constants, partition coefficients (RM values) as a measure for lipophilia, spectra and molecular models of etofenamate are described. Various methods of synthesis of etofenamate and of its intermediates are described. Structural identification is made of by-products simultaneously obtained in the reaction. Pure etofenamate is obtained through repeated molecular distillation. The synthesis is carried out uniformly with protected reaction components and, after splitting off the protective groups, extremely pure etofenamate is obtained. PMID:579118

  16. The experimental study on protective effects and mechanisms of chelating agents of catechols amino carboxylic acid for radiation injury induced by actimides(Th-234)

    International Nuclear Information System (INIS)

    The decorporative efficacy and antioxidative action of prompt and delayed consecutive administration of catecholicpolyaminopolycarboxylate ligands, 7601 and 9501 for radiothorium in mice were investigated. DTPA and Vitamin E were used as positive controls. The competitive abilities of 7601 and 9501 to mobilize the thorium with BSA were studied. Their inhibition effects on superoxide anionas radicals were measured with electron spin resonance. The results showed that 7601 and 9501 are able to effectively prevent the internal radiation injury induced radiothorium, attributing to their double functions of pronounced removal effectiveness and antioxidative action. Their protective effects were better than DTPA and Vitamin E. The mechanisms of protective effects of 7601 and 9501 for internal radiation injury was close related to competitive ability of chelating agent to chelate the thorium with BSA and oxygen free radical scavenging activities

  17. Antifungal agents.

    Science.gov (United States)

    Ryder, N S

    1999-12-01

    At this year's ICAAC Meeting, new data on approximately 20 different antifungal agents were presented, while no new agents were disclosed. Drugs in late development include the triazoles, voriconazole (Pfizer Ltd) and Sch-56592 (Schering-Plough Corp), and the echinocandins, caspofungin (Merck & Co Inc) and FK-463 (Fujisawa Pharmaceutical Co Ltd). In contrast to previous years, presentations on these and earlier developmental compounds were relatively modest in scope, with few significant new data. Little new information appeared on the most recent novel class of agents, the sordarins (Glaxo Wellcome plc). Early clinical results were presented for FK-463, showing acceptable tolerability and dose-dependent efficacy in AIDS-associated esophageal candidiasis. A new liposomal formulation of nystatin (Nyotran; Aronex Pharmaceuticals Inc) was shown to be equivalent to conventional amphotericin B in empiric therapy of presumed fungal infection in neutropenic patients, but with reduced toxicity. Intravenous itraconazole (Janssen Pharmaceutica NV) was an effective prophylactic therapy in invasive pulmonary aspergillosis, while oral itraconazole was discussed as a treatment for fungal infection in heart and liver transplant patients. The allylamine compound, terbinafine (Novartis AG), showed good clinical efficacy against fungal mycetoma, a serious tropical infection. A major highlight was the first presentation of inhibitors of fungal efflux pumps as a strategy for overcoming resistance. MC-510027 (milbemycin alpha-9; Microcide Pharmaceuticals Inc) and its derivatives, potentiated the antifungal activity of triazoles and terbinafine in a number of Candida spp. Another pump inhibitor, MC-005172 (Microcide Pharmaceuticals Inc) showed in vivo potentiation of fluconazole in a mouse kidney infection model. Microcide Pharmaceuticals Inc also presented inhibitors of bacterial efflux pumps. PMID:16113946

  18. Effect of the ulcerogenic agents ethanol, acetylsalicylic acid and taurocholate on actin cytoskeleton and cell motility in cultured rat gastric mucosal cells

    Institute of Scientific and Technical Information of China (English)

    Siamak Bidel; Harri Mustonen; Giti Khalighi-Sikaroudi; Eero Lehtonen; Pauli Puolakkainen; Tuula Kiviluoto; Eero Kivilaakso

    2005-01-01

    AIM: To assess the effects of ulcerogenic agents on actin cytoskeleton and cell motility and the contribution of oxidative stress.METHODS: Rat gastric mucosal cell monolayers were cultured on coverslips. The cells were exposed, with or without allopurinol (2 mmol/L), for 15 min to ethanol (10-150 mL/L), ASA (1-20 mmol/L) or taurocholate (1-20 mmol/L), then the cells were processed for actin and vinculin staining. Cell migration after wounding was also measured.RESULTS: Exposure to 10 mL/L ethanol caused divergence of zonula adherens-associated actin bundles of adjacent cells and decreased rate of migration. These actions were opposed by xanthine oxidase inhibitor allopurinol. Exposure to 50 mL/L ethanol induced degradation and divergence of zonula adherens-associated vinculin from adjacent cells,which was, again, partially reverted by allopurinol. With 1 mmol/L ASA actin filaments became shorter and thicker.However, higher concentrations (10, 20 mmol/L) of ASA returned microfilaments thinner and longer, and decreased rate of migration. Zonula adherens-associated actin bundles were moderately distorted with 10 mmol/L ASA and with 10 mmol/L taurocholate. Exposure to taurocholate provoked changes resembling those of ASA. Taurocholate 5-20 mmol/L decreased the rate of migration dose dependently. The effects of ASA and taurocholate were not prevented by allopurinol.CONCLUSION: All ulcerogenic agents decreased the rate of migration dose dependently and induced divergence of zonula adherens-associated actin bundles of adjacent cells.In addition, ethanol and ASA caused degradation of actin cytoskeleton. Oxidative stress seems to underlie ethanol,but not ASA or taurocholate, induced cytoskeletal damage.

  19. Trading Agents

    CERN Document Server

    Wellman, Michael

    2011-01-01

    Automated trading in electronic markets is one of the most common and consequential applications of autonomous software agents. Design of effective trading strategies requires thorough understanding of how market mechanisms operate, and appreciation of strategic issues that commonly manifest in trading scenarios. Drawing on research in auction theory and artificial intelligence, this book presents core principles of strategic reasoning that apply to market situations. The author illustrates trading strategy choices through examples of concrete market environments, such as eBay, as well as abst

  20. Up-regulation of HLA class-I antigen expression and antigen-specific CTL response in cervical cancer cells by the demethylating agent hydralazine and the histone deacetylase inhibitor valproic acid

    Directory of Open Access Journals (Sweden)

    Lizano-Soberón Marcela

    2006-12-01

    Full Text Available Abstract Background DNA hypermethylation and histone deacetylation are epigenetic events that contribute to the absence or downregulated expression of different components of the tumor recognition complex. These events affect the processing and presentation of antigenic peptides to CTLs by HLA class-I molecules. In this work evaluated the effect of the DNA hypomethylating agent hydralazine and the histone deacetylase inhibitor valproic acid, on the expression of HLA class-I molecules and on the antigen-specific immune recognition of cervical cancer cells. Methods Cell lines C33A (HPV-, CaSki (HPV-16+ and MS751 (HPV-18+ were treated with hydralazine and valproic acid to assess the expression of HLA class-I molecules by flow cytometry and RT-PCR. Promoter methylation of HLA class-I -A, -B and C, was also evaluated by Methylation-Specific PCR. Primary cervical tumors of four HLA-A*0201 allele patients were typed for HPV and their CTL's stimulated in vitro with the T2 cell line previously loaded with 50 μM of the HPV peptides. Cytotoxicity of stimulated CTL's was assayed against Caski and MS751 cells pre-treated with hydralazine and valproic acid. Results Valproic acid and hydralazine/valproic acid up-regulated the constitutive HLA class-I expression as evaluated by flow cytometry and RT-PCR despite constitutive promoter demethylation at these loci. Hydralazine and valproic acid in combination but no IFN-gamma hyperacetylated histone H4 as evaluated by ChiP assay. The antigenic immune recognition of CaSki and MS751 cells by CTLs specific to HPV-16/18 E6 and E7-derived epitopes, was increased by VA and H/VA and the combination of H/VA/IFN-gamma. Conclusion These results support the potential use of hydralazine and valproic acid as an adjuvant for immune intervention in cervical cancer patients whenever clinical protocols based on tumor antigen recognition is desirable, like in those cases where the application of E6 and E7 based therapeutic vaccines

  1. Isolation and screening of lactic acid bacteria and preparation of microbial ecological agents%乳酸菌的分离筛选及其微生态制剂的制备

    Institute of Scientific and Technical Information of China (English)

    刘变芳; 雒丹; 石磊

    2011-01-01

    该研究用市售酸奶中分离纯化到的乳酸菌株和实验室保藏的多种乳酸菌株作为材料,研究不同乳酸菌对大肠杆菌、沙门氏菌、志贺氏菌、金黄色葡萄球菌4种致病菌株的抑菌作用.采用双层平板法从出发菌株中选育到对致病菌株有明显抑制功能的乳酸菌,并将抗菌性能良好的乳酸菌株进行优化组合.组合菌剂转接到脱脂乳中,静置培养48h后,采用真空冷冻干燥技术制备乳酸菌微生态制剂.试验结果表明,从原始菌株中选育到11株对4种致病菌有较强抑制功能的乳酸菌株;优化组合乳酸菌在MRS培养液中,静置培养17h活菌数达到最大值;冷冻干燥过程采用2%麦芽糖作为保护剂,微生态制剂中乳酸菌活菌数为3.36× 105cfu/g,存活率达到68.6%.%Antibacterial effect of lactic acid bacteria purified from yogurt and preserved in our laboratory on pathogenic strains of Higellae pathogenic, Staphylococcus aureus, Salmonella, and Escherichia coli were studied. Double-plate method was adopted to select lactic acid bacteria that had a significant inhibition function on pathogenic strains, and lactic acid bacteria strains with good anti-bacterial performances was combined and optimized. Combined strains were inoculated with skim milk to produce microbial ecological agents of lactic acid bacteria by vacuum freeze-drying after 48h static culture. The experimental results shown that among the original lactic acid bacteria strains, eleven strains had significant inhibition effect on the four pathogenic strains, and the number of optimized combination reach its peak after 17h static culture in MRS medium. When using 2% of maltose as protective agent, the number of survival bacteria was 3.36x105cfu/g, the survival rate of lactic acid bacteria in microbial ecological agents after vacuum freeze-drying could reach 68.6%.

  2. Effect of Sweetening Agents and Hydrocolloids on Rheological Properties of Acid Modified Wheat Starch%甜味料和亲水胶体对酸改性淀粉凝胶粘度及质构的影响

    Institute of Scientific and Technical Information of China (English)

    曾婷婷; 张立彦

    2011-01-01

    The effect of several sweetening agents (sucrose, glucose, sorbitol, maltitol, isomaltitol) and hydrocolloids (konjac gum, agar, gellan gum, alginic acid sodium, tamarind gum, pectin, Arabic gum) on viscidity, gel strength and gel texture of acid modified wheat starch were studied. The results showed that the sequence of cooperating effect of interaction between sweetening agents or hydrocolloid and acid modified wheat starch respectively was: sorbitol>isomaltitol>maltitol>sucrose>glucose; agar>gellan gum>konjac gum>alginic acid sodium>tamarind gum>pectin>Arabic gum. Sorbitol and isomaltitol had higher effects on gel strength of acid modified wheat starch than other sweetening agents. Agar, gellan gum and konjac gum and carrageenan increased the gel strength. The gel texture analysis of acid modified wheat starch showed that the starch had the highest hardness and cohesiveness by adding agar, while it had the best springiness by adding gellan gum.%本文研究了各种甜味料(蔗糖、淀粉糖浆、山梨糖醇、麦芽糖醇、异麦芽糖醇)和亲水胶体(魔芋胶、琼脂、结冷胶、海藻酸钠、罗望子胶、果胶、阿拉伯胶、卡拉胶)对酸改性淀粉糊的粘度、凝胶体强度、质构的影响.结果表明:相同浓度甜味料和不同浓度(0.1%~0.5%)的胶体对酸改性淀粉协同增粘作用的大小顺序分别为:山梨糖醇>异麦芽糖醇>麦芽糖醇>蔗糖>淀粉糖浆,琼脂>结冷胶>魔芋胶>海藻酸钠>罗望子胶>果胶>阿拉伯胶;山梨糖醇和异麦芽糖醇对小麦酸改性淀粉的凝胶强度影响比其他甜味剂对其的影响幅度大;琼脂、结冷胶、魔芋胶和卡拉胶对小麦酸改性淀粉的凝胶强度增强较大;而在质构方面,琼脂对其硬度、内聚性和耐聚性增强最大,而结冷胶对其弹性增强最大.

  3. Effect of a novel insulinotropic agent, succinic acid monoethyl ester, on lipids and lipoproteins levels in rats with streptozotocin-nicotinamideinduced type 2 diabetes

    Indian Academy of Sciences (India)

    Ramalingam Saravanan; Leelavinothan Pari

    2006-12-01

    In the present study, the effect of succinic acid monoethyl ester (EMS) on the pattern of lipids and lipoproteins in streptozotocin-nicotinamide induced type 2 diabetes was investigated. Type 2 diabetes was induced in male Wistar rats by single intraperitoneal injection (i.p.) of 45 mg/kg streptozotocin, 15 min after the i.p administration of 110 mg/kg body weight of nicotinamide. The carboxylic nutrient EMS was administered intraperitonially at a dose of 8 mol/g body weight for 30 days. At the end of experimental period, the effect of EMS on plasma glucose, insulin, thiobarbituric acid reactive substances (TBARS) and hydroperoxide (HP) and serum triglycerides (TG), phospholipids (PL), free fatty acids (FFA), total cholesterol (TC), very low density lipoprotein-cholesterol (VLDL-C) and low density lipoprotein-cholesterol (LDL-C), high-density lipoprotein-cholesterol (HDL-C) and the percentage of antiatherogenic index (AAI) (ratio of HDL-C to total cholesterol) were studied. Administration of EMS to diabetic rats resulted in a significant reduction in the elevated levels of plasma glucose, TBARS and hydroperoxides as well as TG, PL, FFA, TC, VLDL-C and LDC-C levels. The decreased plasma insulin and serum HDL-C and percentage of AAI in diabetic rats were also reversed towards near normal. The effect produced by EMS was compared with metformin, a reference drug. The results indicates that the administration of EMS and metformin to nicotinamide-streptozotocin diabetic rats normalized plasma glucose, insulin concentrations and caused marked improvement in altered lipids, lipoprotein and lipid peroxidation markers during diabetes. Our results show the antihyperlipidemic properties of EMS and metformin in addition to its antidiabetic action. Moreover, the antihyperlipidemic effect could represent a protective mechanism against the development of atherosclerosis.

  4. Comparison of the concentration-effect relationship of a local antiinflammatory agent and oral acetylsalicylic acid: the value of local application.

    Science.gov (United States)

    Poisson, M; Ralambosoa, C; Blehaut, H; Astoin, J

    1985-01-01

    Using a pharmacological model, the comparison between acetylsalicylic acid (ASA), administered orally, and a solution combining two salicylate derivatives (ethyl 5-methoxy-salicylate and 3-phenyl-propyl-salicylate), applied locally, demonstrated the value of the local application. Indeed, the pharmacological activity was highly significant and directly related to the tissue concentration of salicyl ions, which was higher after local application of the solution than after oral administration of ASA. The local solution also resulted in a lower plasma concentration of salicylate ions, allowing high plasma salicylate concentrations to be avoided. PMID:4074414

  5. Okadaic acid

    DEFF Research Database (Denmark)

    Danielsen, E Michael; Hansen, Gert H; Severinsen, Mai C K

    2014-01-01

    Okadaic acid (OA) is a polyether fatty acid produced by marine dinoflagellates and the causative agent of diarrhetic shellfish poisoning. The effect of OA on apical endocytosis in the small intestine was studied in organ cultured porcine mucosal explants. Within 0.5-1 h of culture, the toxin caused...... endosomes (TWEEs) occurred unimpeded in the presence of OA, FM condensed in larger subapical structures by 1 h, implying a perturbed endosomal trafficking/maturation. The fluorescent lysosomotropic agent Lysotracker revealed induction of large lysosomal structures by OA. Endocytosis from the brush border...

  6. Green Route for Efficient Synthesis of Novel Amino Acid Schiff Bases as Potent Antibacterial and Antifungal Agents and Evaluation of Cytotoxic Effects

    Directory of Open Access Journals (Sweden)

    Harshita Sachdeva

    2014-01-01

    Full Text Available Green chemical one-pot multicomponent condensation reaction of substituted 1H-indole-2,3-diones (1, various amino acids (2, and thiosemicarbazide (3 is found to be catalyzed by lemon juice as natural acid using water as a green solvent to give the corresponding Schiff bases (4 in good to excellent yields. This method is experimentally simple, clean, high yielding, and green, with reduced reaction times. The product is purified by simple filtration followed by washing with water and drying process. The synthesized compounds are characterized by FT-IR, 13CNMR, and 1HNMR spectroscopy and are screened for their antifungal activity against Aspergillus niger, Penicillium notatum, Fusarium oxysporum, Alternaria brassicicola, Chaetomium orium, and Lycopodium sp. and antibacterial activity against Gram-positive bacteria, Bacillus licheniformis, Staphylococcus aureus, and Micrococcus luteus, and Gram-negative bacteria, Pseudomonas aeruginosa and Escherichia coli. Compounds have also been evaluated for cytotoxic effects against human colon cancer cell line Colo205.

  7. Gemini Surfactants Based on Bis-Imidazolium Alkoxy Derivatives as Effective Agents for Delivery of Nucleic Acids: A Structural and Spectroscopic Study.

    Directory of Open Access Journals (Sweden)

    Zuzanna Pietralik

    Full Text Available The success rate of gene therapy depends on the efficient transfection of genetic material into cells. The golden mean between harmlessness and high effectiveness can be provided by synthetic lipid-like molecules that are similar to the components of biological membranes. Cationic gemini surfactants are one such moiety and because of their favourable physicochemical properties (double positive electric charge, reduced toxicity, low values of critical micelle concentration, they show great potential as delivery system components for genetic material in gene therapy. The aim of this study was to investigate the process of the complexation of cationic gemini surfactants with nucleic acids: double-stranded DNA of different sizes (21 bp, ~185 bp, ~20 kbp and siRNA (21 bp. The tested series of dicationic surfactants consists of bis-imidazolium quaternary salts with varying lengths of hydrophobic side chains (m = 5, 6, 7, 8, 9, 11, 12, 14, 16. On the basis of the data obtained by circular dichroism spectroscopy and electrophoresis, we concluded that the studied gemini surfactants with long side chains effectively bind nucleic acids at low concentrations, which leads to the formation of stable lipoplexes. Images obtained by atomic force microscopy also confirmed the formation of vesicular structures, i.e., complexes between DNA and surfactants. The cytotoxicity of selected surfactants was also tested on HeLa cells. The surfactant toxicity significantly depends on surfactant geometry (the length of hydrophobic chain.

  8. Synthesis and evaluation of 18 F-labeled bile acid compound: A potential PET imaging agent for FXR-related diseases

    International Nuclear Information System (INIS)

    The farnesoid-X-receptor (FXR) is a member of the nuclear hormone receptor superfamily. The FXR has critical functions in maintaining bile acid synthesis and homeostasis, liver regeneration and tumorigenesis, intestinal diseases, intestinal tumorigenesis, cholesterol gallstone disease, cholestasis, and atherosclerosis. FXR expression is strongly downregulated in liver fibrosis, hepatocellular adenoma and hepatocellular carcinoma compared to expression levels in adjacent normal tissues. Chenodeoxycholic acid (CDCA) is the most potent physiological ligand for FXR. CDCA was radiolabeled with 18 F based on the efficiency click reaction of 1,3-dipolar cycloaddition of terminal alkynes and organic azides for noninvasively evaluating the relationship between FXR and FXR-related disease. The PET tracer [18 F]8 was produced by ‘click’ labeling and showed a high non-decay corrected radiochemical yield (end of synthesis (EOS) yield = 42 ± 3% (n = 5) from aqueous [18 F]fluoride), high radiochemical purity ( > 99%), and high specific activity (> 320 GBq/μmol). [18 F]8 had a high metabolic stability in vitro and in vivo. PET imaging studies in nude mice indicated a rapid uptake of the tracer into liver tissue with uniform distribution of radioactivity in the liver. Significant accumulation of radioactivity was found in the liver, gallbladder, and intestine, while no obvious uptake was observed in other organs, such as the bladder, heart, and brain. Thus, this PET tracer represents a novel tool for early detection of abnormalities in the liver and staging of neoplasms

  9. Gemini Surfactants Based on Bis-Imidazolium Alkoxy Derivatives as Effective Agents for Delivery of Nucleic Acids: A Structural and Spectroscopic Study

    Science.gov (United States)

    Pietralik, Zuzanna; Kołodziejska, Żaneta; Weiss, Marek; Kozak, Maciej

    2015-01-01

    The success rate of gene therapy depends on the efficient transfection of genetic material into cells. The golden mean between harmlessness and high effectiveness can be provided by synthetic lipid-like molecules that are similar to the components of biological membranes. Cationic gemini surfactants are one such moiety and because of their favourable physicochemical properties (double positive electric charge, reduced toxicity, low values of critical micelle concentration), they show great potential as delivery system components for genetic material in gene therapy. The aim of this study was to investigate the process of the complexation of cationic gemini surfactants with nucleic acids: double-stranded DNA of different sizes (21 bp, ~185 bp, ~20 kbp) and siRNA (21 bp). The tested series of dicationic surfactants consists of bis-imidazolium quaternary salts with varying lengths of hydrophobic side chains (m = 5, 6, 7, 8, 9, 11, 12, 14, 16). On the basis of the data obtained by circular dichroism spectroscopy and electrophoresis, we concluded that the studied gemini surfactants with long side chains effectively bind nucleic acids at low concentrations, which leads to the formation of stable lipoplexes. Images obtained by atomic force microscopy also confirmed the formation of vesicular structures, i.e., complexes between DNA and surfactants. The cytotoxicity of selected surfactants was also tested on HeLa cells. The surfactant toxicity significantly depends on surfactant geometry (the length of hydrophobic chain). PMID:26641889

  10. Mycophenolate antagonizes IFN-γ-induced catagen-like changes via β-catenin activation in human dermal papilla cells and hair follicles.

    Science.gov (United States)

    Ryu, Sunhyo; Lee, Yonghee; Hyun, Moo Yeol; Choi, Sun Young; Jeong, Kwan Ho; Park, Young Min; Kang, Hoon; Park, Kui Young; Armstrong, Cheryl A; Johnson, Andrew; Song, Peter I; Kim, Beom Joon

    2014-01-01

    Recently, various immunosuppressant drugs have been shown to induce hair growth in normal hair as well as in alopecia areata and androgenic alopecia; however, the responsible mechanism has not yet been fully elucidated. In this study, we investigate the influence of mycophenolate (MPA), an immunosuppressant, on the proliferation of human dermal papilla cells (hDPCs) and on the growth of human hair follicles following catagen induction with interferon (IFN)-γ. IFN-γ was found to reduce β-catenin, an activator of hair follicle growth, and activate glycogen synthase kinase (GSK)-3β, and enhance expression of the Wnt inhibitor DKK-1 and catagen inducer transforming growth factor (TGF)-β2. IFN-γ inhibited expression of ALP and other dermal papillar cells (DPCs) markers such as Axin2, IGF-1, and FGF 7 and 10. MPA increased β-catenin in IFN-γ-treated hDPCs leading to its nuclear accumulation via inhibition of GSK3β and reduction of DKK-1. Furthermore, MPA significantly increased expression of ALP and other DPC marker genes but inhibited expression of TGF-β2. Therefore, we demonstrate for the first time that IFN-γ induces catagen-like changes in hDPCs and in hair follicles via inhibition of Wnt/β-catenin signaling, and that MPA stabilizes β-catenin by inhibiting GSK3β leading to increased β-catenin target gene and DP signature gene expression, which may, in part, counteract IFN-γ-induced catagen in hDPCs. PMID:25247578

  11. Mycophenolate Antagonizes IFN-γ-Induced Catagen-Like Changes via β-Catenin Activation in Human Dermal Papilla Cells and Hair Follicles

    Directory of Open Access Journals (Sweden)

    Sunhyo Ryu

    2014-09-01

    Full Text Available Recently, various immunosuppressant drugs have been shown to induce hair growth in normal hair as well as in alopecia areata and androgenic alopecia; however, the responsible mechanism has not yet been fully elucidated. In this study, we investigate the influence of mycophenolate (MPA, an immunosuppressant, on the proliferation of human dermal papilla cells (hDPCs and on the growth of human hair follicles following catagen induction with interferon (IFN-γ. IFN-γ was found to reduce β-catenin, an activator of hair follicle growth, and activate glycogen synthase kinase (GSK-3β, and enhance expression of the Wnt inhibitor DKK-1 and catagen inducer transforming growth factor (TGF-β2. IFN-γ inhibited expression of ALP and other dermal papillar cells (DPCs markers such as Axin2, IGF-1, and FGF 7 and 10. MPA increased β-catenin in IFN-γ-treated hDPCs leading to its nuclear accumulation via inhibition of GSK3β and reduction of DKK-1. Furthermore, MPA significantly increased expression of ALP and other DPC marker genes but inhibited expression of TGF-β2. Therefore, we demonstrate for the first time that IFN-γ induces catagen-like changes in hDPCs and in hair follicles via inhibition of Wnt/β-catenin signaling, and that MPA stabilizes β-catenin by inhibiting GSK3β leading to increased β-catenin target gene and DP signature gene expression, which may, in part, counteract IFN-γ-induced catagen in hDPCs.

  12. A Retrospective Comparison of Mycophenolate Mofetil with Low-Exposure Cyclosporine Versus Standard Cyclosporine Therapy in De Novo Liver Transplant Patients.

    Science.gov (United States)

    Senft, Jonas D; Gotthardt, Daniel N; Frischbier, Lina; Bruns, Helge; Schemmer, Peter

    2015-01-01

    BACKGROUND Data on low-exposure calcineurin inhibitor therapy with mycophenolate mofetil (MMF) in de novo liver transplant patients are limited and restricted to tacrolimus. MATERIAL AND METHODS Twenty-eight patients receiving cyclosporine and MMF at a single center were identified retrospectively and categorized as low-exposure or standard-exposure CsA (median concentration <80 ng/mL [n=16] or ≥80 ng/mL [n=12] during days 1-7) and analyzed to 12 weeks post-transplant. RESULTS Biopsy-proven acute rejection (Banff ≥4) occurred in 3 low-CsA patients and no standard-CsA patients (p=0.238); graft failure occurred in 4 and zero patients, respectively (p=0.113); no graft loss was attributable to rejection. Mean (SD) estimated GFR at baseline and week 12 was 79.5 (45.3) and 79.3 (24.5) mL/min/1.73 m2 in the low-CsA group (p=0.508), and 106.0 (66.9) and 86.7 (23.2) mL/min/1.73 m2 in the standard-CsA group (p=0.093). Estimated GFR decreased significantly in patients with good baseline renal function (≥80 mL/min/1.73 m2) in the standard-CsA (p=0.028) and increased markedly in patients with poor function (≤60 mL/min/1.73 m2) given low-CsA (p=0.043). There was no significant between-group difference regarding incidence of infections. CONCLUSIONS These preliminary findings suggest that immunosuppressive efficacy is maintained with low-exposure CsA and MMF in de novo liver transplant patients and good baseline renal function may be better preserved, but no benefit for infections was observed. PMID:26364728

  13. Mycophenolate mofetil and curcumin provide comparable therapeutic benefit in experimental chronic kidney disease: role of Nrf2-Keap1 and renal dopamine pathways.

    Science.gov (United States)

    Tapia, Edilia; García-Arroyo, Fernando; Silverio, Octaviano; Rodríguez-Alcocer, Alma N; Jiménez-Flores, Ana B; Cristobal, Magdalena; Arellano, Abraham S; Soto, Virgilia; Osorio-Alonso, Horacio; Molina-Jijón, Eduardo; Pedraza-Chaverri, José; Sanchez-Lozada, Laura G

    2016-07-01

    Increased oxidative stress and inflammation have an important role in the pathophysiology of chronic kidney disease (CKD). On the other hand, more affordable therapeutic alternatives for treating this disease are urgently needed. Therefore, we compared the therapeutic efficacy of curcumin and mycophenolate mofetil (MMF) in 5/6 nephrectomy (5/6 Nx) model of CKD. Also, we evaluated whether both compounds provide benefit through the preservation of similar antioxidant mechanisms. Four groups of male Wistar were studied over a period of 4 wk. Control sham group (n= 12), 5/6 Nx (n = 12), 5/6 Nx + MMF (30 mg/k BW/day, n = 11) and 5/6 Nx + Curcumin (120 mg/k BW/day, n = 12). Renal function and markers of oxidative stress and inflammation were evaluated. Also Nrf2-Keap1 and renal dopamine, antioxidant pathways were assessed. 5/6 Nx induced an altered renal autoregulation response, proteinuria, and hypertension; these effects were in association with increased oxidative stress, endothelial dysfunction and renal inflammation. The mechanisms associated with these alterations included a reduced nuclear translocation of Nrf2 and hyperphosphorylation of dopamine D1 receptor with a concurrent overactivation of renal NADPH oxidase. Treatments with MMF and curcumin provided equivalent therapeutic efficacy as both prevented functional renal alterations as well as preserved antioxidant capacity and avoided renal inflammatory infiltration. Moreover, both treatments preserved Nrf2-Keap1 and renal dopamine antioxidant pathways. In summary, therapeutic strategies aimed to preserve renal antioxidant pathways can help to retard the progression of CKD. PMID:27050624

  14. Study on the preparation of 99mTc=3- bromo-2, 4, 6-Trimethylacetanilidoiminodiacetic Acid (Br-IDA) as a hepatobiliary imaging agent

    International Nuclear Information System (INIS)

    Br-IDA compound is used for in vivo diagnotic application in nuclar medicine as hepatobiliary imaging agent after being labelled with 99m Tc. A high labelling yield (>97%) and a high in vitro stability (= 95% after 5 h) were achieved by reduction of heptavalent 99m TcO4 which eluted under aseptic conditions from commercially available 99 Mo/99m Tc generator. The stannous reduction method for formation of 99m Tc-Br-IDA complex was used. The different parameters affecting the labelling yield are studied in order to optimize the labelling yield. These factors are the amount of ligand, the Sn(II) content, the pH of reaction mixture and reaction time. The radiochemical purity of 99m Tc-Br-IDA complex was examined by high performance liquid chrimatography (HPLC) and instant thin layer chromatography (ITLC). 99m Tc-Br-IDA complex was rapidly excreted via the hepatocytes with fast liver clearance and minimum urinary excretion (>75% of the activity was found in the gastrointestinal system and < 5% in the kidney, at one hour post injection in mice)

  15. Radioprotective Agents

    Directory of Open Access Journals (Sweden)

    Ilker Kelle

    2008-01-01

    Full Text Available Since1949, a great deal of research has been carried out on the radioprotective activity of various chemical substances. Thiol compounds, compounds which contain –SH radical, different classes of pharmacological agents and other compounds such as vitamine C and WR-2721 have been shown to reduce mortality when administered prior to exposure to a lethal dose of radiation. Recently, honey bee venom as well as that of its components melittin and histamine have shown to be valuable in reduction of radiation-induced damage and also provide prophylactic alternative treatment for serious side effects related with radiotherapy. It has been suggested that the radioprotective activity of bee venom components is related with the stimulation of the hematopoetic system.

  16. β–Cyclodextrin–Propyl Sulfonic Acid Catalysed One-Pot Synthesis of 1,2,4,5-Tetrasubstituted Imidazoles as Local Anesthetic Agents

    Directory of Open Access Journals (Sweden)

    Yan Ran

    2015-11-01

    Full Text Available Some functionalized 1,2,4,5-tetrasubstituted imidazole derivatives were synthesized using a one-pot, four component reaction involving 1,2-diketones, aryl aldehydes, ammonium acetate and substituted aromatic amines. The synthesis has been efficiently carried out in a solvent free medium using β-cyclodextrin-propyl sulfonic acid as a catalyst to afford the target compounds in excellent yields. The local anesthetic effect of these derivatives was assessed in comparison to lidocaine as a standard using a rabbit corneal and mouse tail anesthesia model. The three most potent promising compounds were subjected to a rat sciatic nerve block assay where they showed considerable local anesthetic activity, along with minimal toxicity. Among the tested analogues, 4-(1-benzyl-4,5-diphenyl-1H-imidazol-2-yl-N,N-dimethylaniline (5g was identified as most potent analogue with minimal toxicity. It was further characterized by a more favourable therapeutic index than the standard.

  17. Synthesis and Characterization of Poly(hydroxyethyl methacrylate-co-methacrylic acid) Cross Linked Polymeric Network for the Delivery of Analgesic Agent

    International Nuclear Information System (INIS)

    Objective of the study was to synthesize a chemically cross-linked poly(hydroxyethylmethacrylate-co-methacrylic acid) hydrogel (p(HEMA-co-MAA hydrogel)) for pH-responsive, controlled drug delivery of Flurbiprofen. pH-sensitive hydrogel drug delivery system was synthesized with the help of poly hydroxyethyl methacrylate (HEMA) and methacrylic acid (MAA) by using ethylene glycol dimethacrylate (EGDMA) as crosslinker. The monomers (HEMA and MAA) were successfully cross linked through free radical polymerization process, initiated by benzoyl peroxide in an aqueous medium. All formulations were loaded with Flurbiprofen as a model drug and evaluated at pH 1.2 and pH 7.4 to investigate pH-responsive nature of the system. Fourier transform infrared spectroscopy (FTIR) was performed to confirm the cross-linking of copolymer while thermo gravimetric analysis (TGA) and differential scanning calorimetry (DSC) were performed to evaluate the thermal stability of the system. Swelling studies and in-vitro release studies were carried out to evaluate pH-responsive nature of the hydrogels. FTIR confirmed that monomers were successfully cross-linked to form a copolymer. Hydrogel system showed less swelling at lower pH while at higher pH, it showed higher swelling, releasing drug in the same fashion. It was concluded that a stable hydrogel network was chemically cross-linked showing pH-responsive nature and thus, synthesized p(HEMA-co-MAA) hydrogels can be successfully employed as potential candidate for controlled drug delivery. (author)

  18. An agent framework for dynamic agent retraining: Agent academy

    OpenAIRE

    Mitkas, P.; A. Symeonidis; Kechagias, D.; Athanasiadis, I.N.; Laleci, G.; KURT, G.; Kabak, Y.; Acar, A.; Dogac, A.

    2004-01-01

    Agent Academy (AA) aims to develop a multi-agent society that can train new agents for specific or general tasks, while constantly retraining existing agents in a recursive mode. The system is based on collecting information both from the environment and the behaviors of the acting agents and their related successes/failures to generate a body of data, stored in the Agent Use Repository, which is mined by the Data Miner module, in order to generate useful knowledge about the application domai...

  19. A 3D QSAR Study of Betulinic Acid Derivatives as Anti-Tumor Agents Using Topomer CoMFA: Model Building Studies and Experimental Verification

    Directory of Open Access Journals (Sweden)

    Yang Wang

    2013-08-01

    Full Text Available Betulinic acid (BA is a natural product that exerts its cytotoxicity against various malignant carcinomas without side effects by triggering the mitochondrial pathway to apoptosis. Betulin (BE, the 28-hydroxyl analog of BA, is present in large amounts (up to 30% dry weight in the outer bark of birch trees, and shares the same pentacyclic triterpenoid core as BA, yet exhibits no significant cytotoxicity. Topomer CoMFA studies were performed on 37 BA and BE derivatives and their in vitro anti-cancer activity results (reported as IC50 values against HT29 human colon cancer cells in the present study. All derivatives share a common pentacyclic triterpenoid core and the molecules were split into three pieces by cutting at the C-3 and C-28 sites with a consideration toward structural diversity. The analysis gave a leave-one-out cross-validation q2 value of 0.722 and a non-cross-validation r2 value of 0.974, which suggested that the model has good predictive ability (q2 > 0.2. The contour maps illustrated that bulky and electron-donating groups would be favorable for activity at the C-28 site, and a moderately bulky and electron-withdrawing group near the C-3 site would improve this activity. BE derivatives were designed and synthesized according to the modeling result, whereby bulky electronegative groups (maleyl, phthalyl, and hexahydrophthalyl groups were directly introduced at the C-28 position of BE. The in vitro cytotoxicity values of the given analogs against HT29 cells were consistent with the predicted values, proving that the present topomer CoMFA model is successful and that it could potentially guide the synthesis of new betulinic acid derivatives with high anti-cancer activity. The IC50 values of these three new compounds were also assayed in five other tumor cell lines. 28-O-hexahydrophthalyl BE exhibited the greatest anti-cancer activities and its IC50 values were lower than those of BA in all cell lines, excluding DU145 cells.

  20. Aqueous two-phase system cold-set gelation using natural and recombinant probiotic lactic acid bacteria as a gelling agent.

    Science.gov (United States)

    Léonard, Lucie; Husson, Florence; Langella, Philippe; Châtel, Jean-Marc; Saurel, Rémi

    2016-05-01

    The present study aimed to entrap probiotic lactic acid bacteria (LAB) in a sodium alginate and sodium caseinate aqueous two-phase gel system. The natural acidifying properties of two therapeutic probiotic LAB were exploited to liberate calcium ions progressively from calcium carbonate (CaCO3), which caused the gelation of the co-existing phases. Bi-biopolymeric matrix gelation of GDL/CaCO3 or LAB/CaCO3 was monitored by dynamic rheological measurements, and the final gels were characterized by frequency dependence measurements and confocal laser scanning microscopy. Weak to strong gels were formed with an elastic modulus G' from 10 to 1.000Pa, respectively. After cold-set gelation of our system, confocal laser scanning microscopy showed spherical protein microdomains trapped within a calcium alginate network. LAB cells were stained to study their partition in the self-gelling matrices. Our LAB strains showed two different behaviors, which may relate to the exopolysaccharide production: (i) Lactobacillus plantarum CNRZ1997 cells were found mainly in continuous alginate networks, whereas (ii) Lactococcus lactis cells were localized in protein microdomains. This alginate-caseinate phase-separated system that was self-gelled by LAB cells may be an innovative approach for immobilizing and protecting LAB cells. PMID:26874119

  1. Inhibition of para-Hydroxyphenylpyruvate Dioxygenase by Analogues of the Herbicide Nitisinone As a Strategy to Decrease Homogentisic Acid Levels, the Causative Agent of Alkaptonuria.

    Science.gov (United States)

    Laschi, Marcella; Bernardini, Giulia; Dreassi, Elena; Millucci, Lia; Geminiani, Michela; Braconi, Daniela; Marzocchi, Barbara; Botta, Maurizio; Manetti, Fabrizio; Santucci, Annalisa

    2016-04-01

    Alkaptonuria (AKU) is a rare multisystem metabolic disease caused by deficient activity of homogentisate 1,2-dioxygenase (HGD), which leads to the accumulation of homogentisic acid (HGA). Currently, there is no treatment for AKU. The sole drug with some beneficial effects is the herbicide nitisinone (1), an inhibitor of p-hydroxyphenylpyruvate dioxygenase (4-HPPD). 1 has been used as a life-saving drug in infants with type I tyrosinemia despite severe side effects due to the buildup of tyrosine. Four clinical trials of nitisinone to treat AKU have shown that 1 consistently decreases HGA levels, but also caused the accumulation of tyrosine in blood serum. Moreover, the human preclinical toxicological data for 1 are incomplete. In this work, we performed pharmacodynamics and toxicological evaluations of 1, providing the first report of LD50 values in human cells. Intracellular tyrosinemia was also evaluated. Three additional 4-HPPD inhibitors with a more favorable profile than that of 1 in terms of IC50 , LD50 , and tyrosine accumulation were also identified among commercially available compounds. These may be promising starting points for the development of new therapeutic strategies for the treatment of AKU. PMID:26947423

  2. Vibrational spectroscopic investigation and normal coordinate analysis of the fibrate hypolipidemic agent 5-(2,5-dimethylphenoxy)-2,2-dimethyl pentanoic acid (Gemfibrozil)

    Science.gov (United States)

    Priya, M. Siva; Benitta, T. Asenath; James, C.

    2011-03-01

    Colorless crystals of 5-(2,5-dimethylphenoxy)-2,2-dimethyl pentanoic acid were grown by slow evaporation method and the FT-IR and FT-Raman spectra of the sample were recorded in the region 4000-450 cm -1 and 4000-50 cm -1 respectively. Molecular structure is optimized with the help of B3LYP/6-31G (d) density functional theory method. Stability of the molecule arising from hyperconjugation and charge delocalization is confirmed by the natural bond orbital analysis (NBO). The results show that electron density (ED) in the σ ∗ antibonding orbitals and E (2) energies confirms the occurrence of intra-molecular charge transfer (ICT) within the molecule. The assignments of the vibrational spectra have been carried out with the help of Normal coordinate analysis following the scaled quantum mechanical force field (SQMFF) methodology. Mulliken population analysis on atomic charges is also calculated. The calculated HOMO and LUMO energy gap shows that charge transfer occurs within the molecule.

  3. Facilitated transport of Cr(III) through activated composite membrane containing di-(2-ethylhexyl)phosphoric acid (DEHPA) as carrier agent

    International Nuclear Information System (INIS)

    The facilitated transport of chromium(III) through activated composite membrane (ACM) containing di-(2-ethylhexyl) phosphoric acid (DEHPA) was investigated. DEHPA was immobilised by interfacial polymerisation on polysulfone layer which was deposited on non-woven fabric by using spin coater. Then, ACM was characterised by using scanning electron microscopy (SEM), contact angle measurements and atomic force microscopy (AFM). Initially, batch experiments of liquid-liquid distribution of Cr(III) and the extractant (DEHPA) were carried out to determine the appropriate pH of the feed phase and the results showed that maximum extraction of Cr(III) was achieved at a pH of 4. It was also found that Cr(III) and DEHPA reacted in 1/1 molar ratio. The effects of Cr(III) (in feed phase), HCl (in stripping phase) and DEHPA (in ACM) concentrations were investigated. DEHPA concentration varies from 0.1 to 1.0 M and it was determined that the transport of Cr(III) increased with the carrier concentration up to 0.8 M. It was also observed that the transport of Cr(III) through the ACM tended to increase with Cr(III) and HCl concentrations. The stability of ACM was also confirmed with replicate experiments.

  4. The Different Sensitive Behaviors of a Hydrogen-Bond Acidic Polymer-Coated SAW Sensor for Chemical Warfare Agents and Their Simulants

    Directory of Open Access Journals (Sweden)

    Yin Long

    2015-07-01

    Full Text Available A linear hydrogen-bond acidic (HBA linear functionalized polymer (PLF, was deposited onto a bare surface acoustic wave (SAW device to fabricate a chemical sensor. Real-time responses of the sensor to a series of compounds including sarin (GB, dimethyl methylphosphonate (DMMP, mustard gas (HD, chloroethyl ethyl sulphide (2-CEES, 1,5-dichloropentane (DCP and some organic solvents were studied. The results show that the sensor is highly sensitive to GB and DMMP, and has low sensitivity to HD and DCP, as expected. However, the sensor possesses an unexpected high sensitivity toward 2-CEES. This good sensing performance can’t be solely or mainly attributed to the dipole-dipole interaction since the sensor is not sensitive to some high polarity solvents. We believe the lone pair electrons around the sulphur atom of 2-CEES provide an electron-rich site, which facilitates the formation of hydrogen bonding between PLF and 2-CEES. On the contrary, the electron cloud on the sulphur atom of the HD molecule is offset or depleted by its two neighbouring strong electron-withdrawing groups, hence, hydrogen bonding can hardly be formed.

  5. The Different Sensitive Behaviors of a Hydrogen-Bond Acidic Polymer-Coated SAW Sensor for Chemical Warfare Agents and Their Simulants.

    Science.gov (United States)

    Long, Yin; Wang, Yang; Du, Xiaosong; Cheng, Luhua; Wu, Penglin; Jiang, Yadong

    2015-01-01

    A linear hydrogen-bond acidic (HBA) linear functionalized polymer (PLF), was deposited onto a bare surface acoustic wave (SAW) device to fabricate a chemical sensor. Real-time responses of the sensor to a series of compounds including sarin (GB), dimethyl methylphosphonate (DMMP), mustard gas (HD), chloroethyl ethyl sulphide (2-CEES), 1,5-dichloropentane (DCP) and some organic solvents were studied. The results show that the sensor is highly sensitive to GB and DMMP, and has low sensitivity to HD and DCP, as expected. However, the sensor possesses an unexpected high sensitivity toward 2-CEES. This good sensing performance can't be solely or mainly attributed to the dipole-dipole interaction since the sensor is not sensitive to some high polarity solvents. We believe the lone pair electrons around the sulphur atom of 2-CEES provide an electron-rich site, which facilitates the formation of hydrogen bonding between PLF and 2-CEES. On the contrary, the electron cloud on the sulphur atom of the HD molecule is offset or depleted by its two neighbouring strong electron-withdrawing groups, hence, hydrogen bonding can hardly be formed. PMID:26225975

  6. Retarded acid emulsion

    Energy Technology Data Exchange (ETDEWEB)

    Fast, C.R.; Rixe, F.H.; Duffield, E.L. Jr.

    1972-08-01

    Compositions for use in acidizing hydrocarbon-bearing formations are described. Retarded acid emulsions of prolonged stability make it possible for the acid in this form to be displaced substantial distances out into the formation before becoming spent. The action of acid emulsions for use in acidizing hydrocarbon-bearing formations is prolonged by employing as the principal emulsifying agent an amine salt of dodecylbenzene sulfonic acid. Acid emulsions employing the amine salt of dodecylbenzene sulfonic acid exhibit greater stability than those employing the free acid. (8 claims)

  7. A novel naturally occurring salicylic acid analogue acts as an anti-inflammatory agent by inhibiting nuclear factor-kappaB activity in RAW264.7 macrophages.

    Science.gov (United States)

    Zhang, Tiantai; Sun, Lan; Liu, Rui; Zhang, Dan; Lan, Xi; Huang, Chao; Xin, Wenyu; Wang, Chao; Zhang, Dongming; Du, Guanhua

    2012-03-01

    Methyl salicylate 2-O-β-D-lactoside (DL0309), is a molecule chemically related to salicylic acid that is isolated from Gaultheria yunnanensis (FRANCH.) REHDER (G. yunnanensis). G. yunnanensis, a traditional Chinese herbal medicine, is widely used for treating rheumatoid arthritis, swelling, pain, trauma, and chronic tracheitis. In the present study, we explored the mechanism whereby DL0309 exerts anti-inflammatory effects, using the model of lipopolysaccharide (LPS)-treated RAW264.7 cells. We examined the effects of DL0309 on LPS-induced nuclear factor-kappaB (NF-κB) activity by Western blot analysis, cell imaging analysis and an electrophoretic mobility shift assay (EMSA). Production of pro-inflammatory cytokines was also measured. Our observations indicate that DL0309 suppressed production of nitric oxide (NO), reactive oxygen species (ROS) and the pro-inflammatory cytokines, such as tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), and interleukin-1β (IL-1β), in a concentration-dependent manner. The phosphorylation of IKK-β and degradation of IκB-α by LPS were both inhibited by DL0309 in the cytoplasm. The increased protein level of NF-κB by LPS in the nucleus was also reduced by DL0309. Consistent with these results, we found that DL0309 prevents the nuclear translocation and DNA binding activity of NF-κB. Finally, our results demonstrate that DL0309 exerts anti-inflammatory effects, by inhibiting the production of pro-inflammatory cytokines and suppressing of the activation of the NF-κB signaling pathway in LPS-treated macrophage cells. Therefore, DL0309 may have therapeutic potential for treating inflammatory diseases by regulating the NF-κB pathway and pro-inflammatory cytokine production. PMID:22292506

  8. Novel electrospun nanofibrous matrices prepared from poly(lactic acid)/poly(butylene adipate) blends for controlled release formulations of an anti-rheumatoid agent.

    Science.gov (United States)

    Siafaka, Panoraia I; Barmbalexis, Panagiotis; Bikiaris, Dimitrios N

    2016-06-10

    In the present work, a series of novel formulations consisting of poly(lactic acid)/poly(butylene adipate) (PLA/PBAd) electrospun blends was examined as controlled release matrices for Leflunomide's active metabolite, Teriflunomide (TFL). The mixtures were prepared using different ratios of PLA and PBAd in order to produce nanofibrous matrices with different characteristics. Miscibility studies of the blended polymeric fibers were performed through differential scanning calorimetry (DSC) and X-ray diffractometry (XRD). Hydrolytic degradation in the prepared fibers was evaluated at 37°C using a phosphate buffered saline solution. Different concentrations of (TFL) (5, 10, 15wt.%) were incorporated into nanofibers for examining the drug release behavior in simulated body fluids (SBF), at 37°C. The drug-loaded nanofibrous formulations were further characterized by Fourier Transform Infrared Spectroscopy (FTIR) spectroscopy, DSC and XRD. Gel permeation chromatography (GPC) analysis was used to evaluate the mechanism of TFL release. Artificial neural networks (ANN) and multi-linear-regression (MLR) models were used to evaluate the effect of % content of PBAd (X1) and TFL (X2) on an initial burst effect and a dissolution behavior. It was found that PLA/PBAd nanofibers have different diameters depending on the ratio of used polyesters and added drug. TFL was incorporated in an amorphous form inside the polymeric nanofibers. In vitro release studies reveal that a drug release behavior is correlated with the size of the nanofibers, drug loading and matrix degradation after a specific time. ANN dissolution modeling showed increased correlation efficacy compared to MLR. PMID:27039136

  9. Complexes of Silver(I Ions and Silver Phosphate Nanoparticles with Hyaluronic Acid and/or Chitosan as Promising Antimicrobial Agents for Vascular Grafts

    Directory of Open Access Journals (Sweden)

    Vojtech Adam

    2013-06-01

    Full Text Available Polymers are currently widely used to replace a variety of natural materials with respect to their favourable physical and chemical properties, and due to their economic advantage. One of the most important branches of application of polymers is the production of different products for medical use. In this case, it is necessary to face a significant disadvantage of polymer products due to possible and very common colonization of the surface by various microorganisms that can pose a potential danger to the patient. One of the possible solutions is to prepare polymer with antibacterial/antimicrobial properties that is resistant to bacterial colonization. The aim of this study was to contribute to the development of antimicrobial polymeric material ideal for covering vascular implants with subsequent use in transplant surgery. Therefore, the complexes of polymeric substances (hyaluronic acid and chitosan with silver nitrate or silver phosphate nanoparticles were created, and their effects on gram-positive bacterial culture of Staphylococcus aureus were monitored. Stages of formation of complexes of silver nitrate and silver phosphate nanoparticles with polymeric compounds were characterized using electrochemical and spectrophotometric methods. Furthermore, the antimicrobial activity of complexes was determined using the methods of determination of growth curves and zones of inhibition. The results of this study revealed that the complex of chitosan, with silver phosphate nanoparticles, was the most suitable in order to have an antibacterial effect on bacterial culture of Staphylococcus aureus. Formation of this complex was under way at low concentrations of chitosan. The results of electrochemical determination corresponded with the results of spectrophotometric methods and verified good interaction and formation of the complex. The complex has an outstanding antibacterial effect and this effect was of several orders higher compared to other

  10. Effect of acid or alkaline catalyst and of different capping agents on the optical properties of CdS nanoparticles incorporated within a diureasil hybrid matrix

    Science.gov (United States)

    Gonçalves, Luis F. F. F.; Silva, Carlos J. R.; Kanodarwala, Fehmida K.; Stride, John A.; Pereira, Mario R.

    2015-11-01

    CdS nanoparticles (NPs) were synthesized using colloidal methods and incorporated within a diureasil hybrid matrix. The surface capping of the CdS NPs by 3-mercaptopropyltrimethoxysilane (MPTMS) and 3-aminopropyltrimethoxysilane (APTMS) organic ligands during the incorporation of the NPs within the hybrid matrix has been investigated. The matrix is based on poly(ethylene oxide)/poly(propylene oxide) chains grafted to a siliceous skeleton through urea bonds and was produced by sol-gel process. Both alkaline and acidic catalysis of the sol-gel reaction were used to evaluate the effect of each organic ligand on the optical properties of the CdS NPs. The hybrid materials were characterized by absorption, steady-state and time-resolved photoluminescence spectroscopy and High Resolution Transmission Electron Microscopy (HR-TEM). The preservation of the optical properties of the CdS NPs within the diureasil hybrids was dependent on the experimental conditions used. Both organic ligands (APTMS and MPTMS) demonstrated to be crucial in avoiding the increase of size distribution and clustering of the NPs within the hybrid matrix. The use of organic ligands was also shown to influence the level of interaction between the hybrid host and the CdS NPs. The CdS NPs showed large Stokes shifts and long average lifetimes, both in colloidal solution and in the xerogels, due to the origin of the PL emission in surface states. The CdS NPs capped with MPTMS have lower PL lifetimes compared to the other xerogel samples but still larger than the CdS NPs in the original colloidal solution. An increase in PL lifetimes of the NPs after their incorporation within the hybrid matrix is related to interaction between the NPs and the hybrid host matrix.

  11. Influence of Chelating Agents on Chromium Fate in Sediment

    Institute of Scientific and Technical Information of China (English)

    WANGXIAOCHANG; SUNJINHE; 等

    1996-01-01

    A laboratory investigation on reaction between chelating agents and chromium was conducted to evaluate the effect of chelating agents on the adsorption and desorption of chromium in sediment.The amount of adsorbed chromium(VI) in sediment decreased slightly by 5%-10% because of addition of chelating agents.Chelating agents inhibited the removal of Cr(Ⅲ)by sediment from solutions and the inhibiting effect was in the order:citric acid>tartaric acid>EDTA,Salicylic acid.No effect of chelating agents on desorption of chromium in sediment was observed.

  12. PENGGUNAAN BERBAGAI JENIS BAHAN PELINDUNG UNTUK MEMPERTAHANKAN VIABILITAS BAKTERI ASAM LAKTAT YANG DI ISOLASI DARI AIR SUSU IBU PADA PROSES PENGERINGAN BEKU [Utilization of various cryogenic agents during freeze drying to Maintain the viability of Lactic Acid Bacteria Isolated from breast milk

    Directory of Open Access Journals (Sweden)

    Ni Nyoman Puspawati1*

    2010-06-01

    Full Text Available Lactic acid bacteria are the most important bacteria having potential as probiotic. The objectives of the present study were to examine the growth of Lactic Acid Bacteria, identify the Lactic Acid Bacteria capable of surviving and evaluate the best cryogenic agents that protect the viability of Lactic Acid Bacteria during freeze drying. Four cryogenic agents, i.e. sucrose, lactose, skim milk and maltodextrin, were used in freeze drying of three species of Lactic Acid Bacteria, i.e. Pediococcus pentosaceus A16, Lactobacillus brevis A17 and Lactobacillus rhamnosus R21 isolated from breast milk. Evaluation included viability before and after freeze drying, survival of freeze dried culture in 0.5 % bile salt and low pH for 5 hours. The result showed that three of cryogenics, i.e. sucrose, lactose and skim milk improved the viability of freeze dried of all lactobacilli, except maltodextrin that did not give protection to L. rhamnosus R21. Evaluation on the survival of LAB in 0.5 % bile salt showed that cryogenic agents improved the survival rate of all Lactic Acid Bacteria during freeze drying. The cryogenic also improved the survival rate of LAB at low pH, with the best protection given by skim milk on L. rhamnosus R21.

  13. Cyclosporine Plus Methotrexate or Cyclosporine Plus Mycophenolate Mofetil as Graft Versus Host Disease Prophylaxis in Acute Leukemia Transplant: Comparison of Toxicity, Engraftment Kinetics and Transplant Outcome.

    Science.gov (United States)

    Gupta, Alok; Punatar, Sachin; Mathew, Libin; Kannan, Sadhana; Khattry, Navin

    2016-09-01

    We sought to compare two graft-versus-host disease (GVHD) prophylaxis regimen, cyclosporine and methotrexate (CsA+MTX) with CsA+mycophenolate mofetil (MMF) in 77 acute leukemia patients who underwent hematopoietic stem cell transplant (HSCT) between January 2008 and March 2013. Fifty-three patients received CsA+MTX while 24 received CsA+MMF. The incidence of grade 3-4 mucositis and grade 3-4 diarrhea was 74 and 6 % with CsA+MTX compared to 33 % and 21 % with CsA+MMF (P = 0.001 and 0.09 respectively). Forty-two (79 %) patients in CsA+MTX group required total parenteral nutrition compared to 14 (58 %) in CsA+MMF group (P = 0.09). The incidence of engraftment fever was 17 % with CsA+MTX and 41 % with CsA+MMF (P = 0.02). The median time to neutrophil and platelet engraftment was 14 days and 13 days with CsA+MTX compared to 12 days and 10 days with CsA+MMF (P = 0.003 and 0.08 respectively). The incidence of any grade and grade II-IV acute GVHD was 45 and 13 % with CsA+MTX compared to 42 and 29 % with CsA+MMF (P = NS). Incidence of overall and extensive chronic GVHD was 57 and 38 % with CsA+MTX compared to 42 and 17 % with CsA+MMF (P = NS). Incidence of relapse was 38 % with CsA+MTX compared to 33 % with CsA+MMF (P = NS). TRM was 6 % with CsA+MTX and 21 % with CsA+MMF (P = NS). At 2 years, overall survival (OS) was 64 % in CsA+MTX group compared to 46 % in CsA+MMF group (P = NS). We conclude that CsA+MMF is associated with lesser toxicity, faster myeloid engraftment and similar rates of acute and chronic GVHD, TRM, relapse and OS compared to CsA+MTX in acute leukemia transplant. PMID:27429515

  14. Efficacy of a non-hypercalcemic vitamin-D2 derived anti-cancer agent (MT19c and inhibition of fatty acid synthesis in an ovarian cancer xenograft model.

    Directory of Open Access Journals (Sweden)

    Richard G Moore

    Full Text Available BACKGROUND: Numerous vitamin-D analogs exhibited poor response rates, high systemic toxicities and hypercalcemia in human trials to treat cancer. We identified the first non-hypercalcemic anti-cancer vitamin D analog MT19c by altering the A-ring of ergocalciferol. This study describes the therapeutic efficacy and mechanism of action of MT19c in both in vitro and in vivo models. METHODOLOGY/PRINCIPAL FINDING: Antitumor efficacy of MT19c was evaluated in ovarian cancer cell (SKOV-3 xenografts in nude mice and a syngenic rat ovarian cancer model. Serum calcium levels of MT19c or calcitriol treated animals were measured. In-silico molecular docking simulation and a cell based VDR reporter assay revealed MT19c-VDR interaction. Genomewide mRNA analysis of MT19c treated tumors identified drug targets which were verified by immunoblotting and microscopy. Quantification of cellular malonyl CoA was carried out by HPLC-MS. A binding study with PPAR-Y receptor was performed. MT19c reduced ovarian cancer growth in xenograft and syngeneic animal models without causing hypercalcemia or acute toxicity. MT19c is a weak vitamin-D receptor (VDR antagonist that disrupted the interaction between VDR and coactivator SRC2-3. Genome-wide mRNA analysis and western blot and microscopy of MT19c treated xenograft tumors showed inhibition of fatty acid synthase (FASN activity. MT19c reduced cellular levels of malonyl CoA in SKOV-3 cells and inhibited EGFR/phosphoinositol-3kinase (PI-3K activity independently of PPAR-gamma protein. SIGNIFICANCE: Antitumor effects of non-hypercalcemic agent MT19c provide a new approach to the design of vitamin-D based anticancer molecules and a rationale for developing MT19c as a therapeutic agent for malignant ovarian tumors by targeting oncogenic de novo lipogenesis.

  15. Fluid extraction using carbon dioxide and organophosphorus chelating agents

    Science.gov (United States)

    Smart, Neil G.; Wai, Chien M.; Lin, Yuehe; Kwang, Yak Hwa

    1998-01-01

    Methods for extracting metalloid and metal species from a solid or liquid material by exposing the material to a fluid solvent, particularly supercritical CO.sub.2, and a chelating agent are described. The chelating agent forms a chelate with the species, the chelate being soluble in the fluid to allow removal of the species from the material. In preferred embodiments the extraction solvent is supercritical CO.sub.2 and the chelating agent comprises an organophosphorous chelating agent, particularly sulfur-containing organophosphorous chelating agents, including mixtures of chelating agents. Examples of chelating agents include monothiophosphinic acid, di-thiophosphinic acid, phosphine sulfite, phosphorothioic acid, and mixtures thereof. The method provides an environmentally benign process for removing metal and metalloids from industrial waste solutions, particularly acidic solutions. Both the chelate and the supercritical fluid can be regenerated and the contaminant species recovered to provide an economic, efficient process.

  16. Agent Chameleons: Virtual Agents Real Intelligence

    OpenAIRE

    O'Hare, Gregory; Duffy, Brian; Schoen-Phelan, Bianca; Martin, Alan; Bradley, John

    2003-01-01

    Agent Chameleons provides virtual agents powered by real intelligence, delivering next generation autonomic entities that can seamlessly migrate, mutate and evolve on their journey between and within physical and digital information spaces.

  17. 采用钠盐调酸发酵生产D乳酸的工艺研究%Production of D-lactic Acid Using Sodium Hydroxide as Neutralizing Agent

    Institute of Scientific and Technical Information of China (English)

    李媛; 徐书景; 张庆; 王丽敏; 于波; 鞠建松; 赵宝华

    2014-01-01

    Efficient D-lactate production by S porolactobacillus sp .strain CASD using sodium hydroxide as neutralizing agent was demonstrated .High D-lactate production (118 .2 g/L) was achieved using peanut meal as the sole nitrogen source in fed-batch fermentation , with the conversion rate from glucose at 89 .1% and the optical purity at 99 .3 % w hich meets the requirements for polymerization of lactic acid . T he NaO H-based fermentation strategy employed here is suitable for separation of lactic acid by electrodi-alysis .Thus ,the production of high concentration of optically pure D-lactate from cheap substrates ,with the NaO H-based fermentation strategy ,has laid a technical foundation for developing a new cost-effective and integrated method for continuous fermentation of D-lactate coupled with separation .%对芽孢乳杆菌CASD采用钠盐调酸发酵生产 D 乳酸的工艺进行了探索.以廉价花生粕为唯一氮源,采用氢氧化钠为中和剂,D 乳酸的发酵质量浓度达到118.2 g/L ,糖酸转化率为89.1%,光学纯度达到99.3%,满足乳酸聚合要求.钠盐调酸适用于电渗析分离纯化乳酸工艺,该研究为开发新型的连续发酵分离耦合生产 D 乳酸工艺提供了技术基础.

  18. Receiving demulsifying agent from the acid tar

    Energy Technology Data Exchange (ETDEWEB)

    Nikitina, A.A.; Belyaeva, A.S.; Kunakova, R.V. [FGBIHE ' Ufa State Academy of Economics and Services' , Ufa (Russian Federation); Movsumzade, E.M. [FGBIHE ' Ufa State Petroleum Technological Univ.' , Ufa (Russian Federation); Lapidus, A.L. [Russian Academy of Sciences, Moscow (Russian Federation). N.D. Zelinsky Institute of Organic Chemistry

    2012-07-01

    The processing of wastes of petrochemical production makes it possible to reduce the price of produced commodity of petroleum products substantially. Bitumen, fuel oils, tars and other mixture of heavy organic compounds are widely used in road construction, in paint and cable industries, manufacture of roofing materials, are used as boiler and furnace fuel, fuel for marine diesel engines, raw material for the production of modifying additives, fillers, surfaceactive substances, etc. (orig.)

  19. Efeitos de agentes oxidantes e oxigênio dissolvido na descoloração do azo corante acid orange 7 por fotólise e fotocatálise Effects of oxidant agents and dissolved oxygen on the decolorization of acid orange 7 azo dye by photolysis and photocatalysis

    Directory of Open Access Journals (Sweden)

    Adriana Campano Lucilha

    2009-01-01

    Full Text Available The decolorization of acid orange 7 azo dye by photolysis and photocatalysis by ZnO was investigated in the presence of oxidants such as NaClO3, NaBrO3, NaIO4, and K2S2O8 in an open reactor at 30 ºC. The decolorization was relatively fast at lower oxidants concentrations and slow rate at larger concentrations, except for persulfate in the photocatalysis. Concerning photolysis the rate constant enhanced gradually, except for chlorate, outreaching the obtained values by photocatalysis, at higher concentrations. The air saturation decreased the rate constant in both processes and indicated that the azo dye can be decolorized without dissolved oxygen in persulfate medium.

  20. [Anticonvulsant agents in neuralgic pain.].

    Science.gov (United States)

    Jurna, I; Zenz, M

    1992-06-01

    The anticonvulsants, carbamazepine, clonazepam, phenytoin, and valproic acid are capable of depressing attacks of shooting pain in neuralgia. Shooting pain is perceived in trigeminal, intercostal, and other neuralgias, as a consequence of infectious diseases such as herpes zoster, and in the course of polyneuropathies of various causes. It is due to injury of nociceptive afferents, which generate bursts of activity in response to appropriate environmental changes. The anticonvulsant agents have no analgesic property per se, so that background pain remains unchanged. The depression of shooting pain results from the anticonvulsant action of the compounds. Both carbamazepine and phenytoin block synaptic transmission of neuronal hyperactivity by a direct depressant action that includes reduction of sodium conductance and by activation of inhibitory control. Clonazepam and valproic acid act by enhancing GABA-mediated inhibition of synaptic transmission. Carbamazepine is by far the most widely used compound; phenytoin, clonazepam, and valproic acid are not so popular because of their side effects. PMID:18415623

  1. Current methods of the analysis of immunosuppressive agents in clinical materials: A review.

    Science.gov (United States)

    Mika, Adriana; Stepnowski, Piotr

    2016-08-01

    More than 100000 solid organ transplantations are performed every year worldwide. Calcineurin (cyclosporine A, tacrolimus), serine/threonine kinase (sirolimus, everolimus) and inosine monophosphate dehydrogenase inhibitor (mycophenolate mofetil), are the most common drugs used as immunosuppressive agents after solid organ transplantation. Immunosuppressive therapy, although necessary after transplantation, is associated with many adverse consequences, including the formation of secondary metabolites of drugs and the induction of their side effects. Calcineurin inhibitors are associated with nephrotoxicity, cardiotoxicity and neurotoxicity; moreover, they increase the risk of many diseases after transplantation. The review presents a study of the movement of drugs in the body, including the processes of absorption, distribution, localisation in tissues, biotransformation and excretion, and also their accompanying side effects. Therefore, there is a necessity to monitor immunosuppressants, especially because these drugs are characterised by narrow therapeutic ranges. Their incorrect concentrations in a patient's blood could result in transplant rejection or in the accumulation of toxic effects. Immunosuppressive pharmaceuticals are macrolide lactones, peptides, and high molecular weight molecules that can be metabolised to several metabolites. Therefore the two main analytical methods used for their determination are high performance liquid chromatography with various detection methods and immunoassay methods. Despite the rapid development of new analytical methods of analysing immunosuppressive agents, the application of the latest generation of detectors and increasing sensitivity of such methods, there is still a great demand for the development of highly selective, sensitive, specific, rapid and relatively simple methods of immunosuppressive drugs analysis. PMID:26874932

  2. Update on the use of systemic biologic agents in the treatment of noninfectious uveitis

    Directory of Open Access Journals (Sweden)

    Pasadhika S

    2014-02-01

    Full Text Available Sirichai Pasadhika,1 James T Rosenbaum2 1Department of Ophthalmology, Southern Arizona Veterans Administration Health Care System, Tucson, AZ, USA; 2Legacy Devers Eye Institute, Portland, OR, USA Abstract: Uveitis is one of the leading causes of blindness worldwide. Noninfectious uveitis may be associated with other systemic conditions, such as human leukocyte antigen B27-related spondyloarthropathies, inflammatory bowel disease, juvenile idiopathic arthritis, Behçet's disease, and sarcoidosis. Conventional therapy with corticosteroids and immunosuppressive agents (such as methotrexate, azathioprine, mycophenolate mofetil, and cyclosporine may not be sufficient to control ocular inflammation or prevent non-ophthalmic complications in refractory patients. Off-label use of biologic response modifiers has been studied as primary and secondary therapeutic agents. They are very useful when conventional immunosuppressive therapy has failed or has been poorly tolerated, or to treat concomitant ophthalmic and systemic inflammation that might benefit from these medications. Biologic therapy, primarily infliximab, and adalimumab, have been shown to be rapidly effective for the treatment of various subtypes of refractory uveitis and retinal vasculitis, especially Behçet's disease-related eye conditions and the uveitis associated with juvenile idiopathic arthritis. Other agents such as golimumab, abatacept, canakinumab, gevokizumab, tocilizumab, and alemtuzumab may have great future promise for the treatment of uveitis. It has been shown that with proper monitoring, biologic therapy can significantly improve quality of life in patients with uveitis, particularly those with concurrent systemic symptoms. However, given high cost as well as the limited long-term safety data, we do not routinely recommend biologics as first-line therapy for noninfectious uveitis in most patients. These agents should be used with caution by experienced clinicians. The present

  3. [Gastric Acid].

    Science.gov (United States)

    Ruíz Chávez, R

    1996-01-01

    Gastric acid, a product of parietal cells secretion, full fills multiple biological roles which are absolutely necessary to keep corporal homeostasis. The production of the acid depends upon an effector cellular process represented in the first step by histamine, acetilcholine and gastrin, first messengers of the process. These interact with specific receptors than in sequence activate second messengers -cAMP and the calcium-calmodulin system- which afterwards activate a kinase. An specific protein is then phosphorilated by this enzyme, being the crucial factor that starts the production of acid. Finally, a proton bomb, extrudes the acid towards the gastric lumen. The secretion process mentioned above, is progressive lyactivated in three steps, two of which are stimulators -cephalic and gastric phases- and the other one inhibitor or intestinal phase. These stages are started by mental and neurological phenomena -thought, sight, smell or memory-; by food, drugs or other ingested substances; and by products of digestion. Changes in regulation of acid secretion, in the structure of gastro-duodenal mucosal barrier by a wide spectrum of factors and agents including food, drugs and H. pylori, are the basis of acid-peptic disease, entity in which gastric acid plays a fundamental role. From the therapeutic point of view, so at the theoretical as at the practical levels, t is possible to interfere with the secretion of acid by neutralization of some of the steps of the effector cellular process. An adequate knowledge of the basics related to gastric acid, allows to create strategies for the clinical handling of associated pathology, specifically in relation to peptic acid disease in all of the known clinical forms. PMID:12165790

  4. Pharmacologic Agents for Chronic Diarrhea.

    Science.gov (United States)

    Lee, Kwang Jae

    2015-10-01

    Chronic diarrhea is usually associated with a number of non-infectious causes. When definitive treatment is unavailable, symptomatic drug therapy is indicated. Pharmacologic agents for chronic diarrhea include loperamide, 5-hydroxytryptamine type 3 (5-HT3) receptor antagonists, diosmectite, cholestyramine, probiotics, antispasmodics, rifaximin, and anti-inflammatory agents. Loperamide, a synthetic opiate agonist, decreases peristaltic activity and inhibits secretion, resulting in the reduction of fluid and electrolyte loss and an increase in stool consistency. Cholestyramine is a bile acid sequestrant that is generally considered as the first-line treatment for bile acid diarrhea. 5-HT3 receptor antagonists have significant benefits in patients with irritable bowel syndrome (IBS) with diarrhea. Ramosetron improves stool consistency as well as global IBS symptoms. Probiotics may have a role in the prevention of antibiotic-associated diarrhea. However, data on the role of probiotics in the treatment of chronic diarrhea are lacking. Diosmectite, an absorbent, can be used for the treatment of chronic functional diarrhea, radiation-induced diarrhea, and chemotherapy-induced diarrhea. Antispasmodics including alverine citrate, mebeverine, otilonium bromide, and pinaverium bromide are used for relieving diarrheal symptoms and abdominal pain. Rifaximin can be effective for chronic diarrhea associated with IBS and small intestinal bacterial overgrowth. Budesonide is effective in both lymphocytic colitis and collagenous colitis. The efficacy of mesalazine in microscopic colitis is weak or remains uncertain. Considering their mechanisms of action, these agents should be prescribed properly. PMID:26576135

  5. AgentChess : An Agent Chess Approach

    OpenAIRE

    Fransson, Henric

    2003-01-01

    The game of chess has many times been discussed and used for test purpose by science departments of Artificial Intelligence (AI). Although the technique of agent and as well multi-agent systems is quite old, the use of these offspring of AI within chess is limited. This report describes the project performed applying the use of agents to a chess program. To measure the performance of the logic has tests between the developed program main parts been performed. Further tests against a tradition...

  6. Agents in domestic environments

    OpenAIRE

    van Moergestel, Leo; Langerak, Wouter; Meerstra, Glenn; Nieuwenburg, Niels van; Pape, Franc; Telgen, Daniël; Puik, Erik; meyer, john-jules

    2013-01-01

    Athor supplied : "This paper describes an agent-based architecture for domotics. This architecture is based on requirements about expandability and hardware independence. The heart of the system is a multi-agent system. This system is distributed over several platforms to open the possibility to tie the agents directly to the actuators, sensors and devices involved. This way a level of abstraction is created and all intelligence of the system as a whole is related to the agents involved. A pr...

  7. Amino Acid Substitutions in the Cytochrome P-450 Lanosterol 14α-Demethylase (CYP51A1) from Azole-Resistant Candida albicans Clinical Isolates Contribute to Resistance to Azole Antifungal Agents

    OpenAIRE

    Sanglard, Dominique; Ischer, Françoise; Koymans, Luc; Bille, Jacques

    1998-01-01

    The cytochrome P-450 lanosterol 14α-demethylase (CYP51A1) of yeasts is involved in an important step in the biosynthesis of ergosterol. Since CYP51A1 is the target of azole antifungal agents, this enzyme is potentially prone to alterations leading to resistance to these agents. Among them, a decrease in the affinity of CYP51A1 for these agents is possible. We showed in a group of Candida albicans isolates from AIDS patients that multidrug efflux transporters were playing an important role in ...

  8. Culturally Aware Agent Communication

    DEFF Research Database (Denmark)

    Rehm, Matthias; Nakano, Yukiko; Koda, Tomoko;

    2012-01-01

    Agent based interaction in the form of Embodied Conversational Agents (ECAs) has matured over the last decade and agents have become more and more sophisticated in terms of their verbal and nonverbal behavior like facial expressions or gestures. Having such “natural” communication channels...

  9. Riot Control Agents

    Science.gov (United States)

    ... a person has been exposed to riot control agents. Long-term health effects of exposure to riot control agents Prolonged ... person is removed from exposure to riot control agents, long-term health effects are unlikely to occur. How you can ...

  10. Reasoning about emotional agents

    NARCIS (Netherlands)

    Meyer, J.-J.

    2008-01-01

    In this paper we discuss the role of emotions in artificial agent design, and the use of logic in reasoning about the emotional or affective states an agent can reside in. We do so by extending the KARO framework for reasoning about rational agents appropriately. In particular we formalize in this f

  11. Agents modeling agents in information economies

    Energy Technology Data Exchange (ETDEWEB)

    Vidal, J.M.; Durfee, E.H. [Univ. of Michigan, Ann Arbor, MI (United States)

    1996-12-31

    Our goal is to design and build agents that act intelligently when placed in an agent-based information economy, where agents buy and sell services (e.g. thesaurus, search, task planning services, etc.). The economy we are working in is the University of Michigan Digital Library (UMDL), a large scale multidisciplinary effort to build an infrastructure for the delivery of library services. In contrast with a typical economy, an information economy deals in goods and services that are often derived from unique sources (authors, analysts, etc.), so that many goods and services are not interchangeable. Also, the cost of replicating and transporting goods is usually negligible, and the quality of goods and services is difficult to measure objectively: even two sources with essentially the same information might appeal to different audiences. Thus, each agent has its own assessment of the quality of goods and services delivered.

  12. The Possible Role of Transplacentally-Acquired Antibodies to Infectious Agents, With Molecular Mimicry to Nervous System Sialic Acid Epitopes, as Causes of Neuromental Disorders: Prevention and Vaccine Implications

    Directory of Open Access Journals (Sweden)

    André J. Nahmias

    2006-01-01

    Full Text Available Proof of causality of most neuromental disorders (NMD's is largely unavailable. Lessons from four-decade investigations of the epidemiology, immunology, pathogenesis, prevention and therapy of perinatal infectious agents, which invade directly the nervous system, have led us to propose a new indirect effect hypothesis: maternal transplacentally-acquired antibodies, to agents with epitope molecular mimicry with the developing nervous system, can cross the fetus/infant's blood–nervous system barriers to cause NMD's, clinically manifest years later.

  13. Efficacy and safety of a conversion from the original tacrolimus and mycophenolate mofetil to the generics Tacpan® and Mowel® after liver transplantation

    OpenAIRE

    Vollmar, Johanna; Bellmann, Maren Christina; Darstein, Felix; Hoppe-Lotichius, Maria; Mittler, Jens; Heise, Michael; Rüttger, Bernd; Weyer, Veronika; Zimmermann, Anca; Lang, Hauke; Peter R. Galle; Zimmermann, Tim

    2015-01-01

    Background Expensive pharmaceuticals are a major reason for cost intensive health care systems. Long-term immunosuppressive therapy plays a relevant role after organ transplantation. Patents of original drugs have expired and cheaper products are available. Little data are available regarding efficacy and safety of generic immunosuppressive agents. Methods In this prospective study, 25 patients, who were clinically stable for a minimum of 2 years after liver transplantation, were converted fr...

  14. Chemical crowd control agents.

    Science.gov (United States)

    Menezes, Ritesh G; Hussain, Syed Ather; Rameez, Mansoor Ali Merchant; Kharoshah, Magdy A; Madadin, Mohammed; Anwar, Naureen; Senthilkumaran, Subramanian

    2016-03-01

    Chemical crowd control agents are also referred to as riot control agents and are mainly used by civil authorities and government agencies to curtail civil disobedience gatherings or processions by large crowds. Common riot control agents used to disperse large numbers of individuals into smaller, less destructive, and more easily controllable numbers include chloroacetophenone, chlorobenzylidenemalononitrile, dibenzoxazepine, diphenylaminearsine, and oleoresin capsicum. In this paper, we discuss the emergency medical care needed by sufferers of acute chemical agent contamination and raise important issues concerning toxicology, safety and health. PMID:26658556

  15. Decontamination Data - Blister Agents

    Data.gov (United States)

    U.S. Environmental Protection Agency — Decontamination efficacy data for blister agents on various building materials using various decontamination solutions This dataset is associated with the following...

  16. Coating agents affected toward magnetite nanoparticles properties

    Science.gov (United States)

    Petcharoen, Karat; Sirivat, Anuvat

    2012-02-01

    Magnetite nanoparticles --MNPs-- are innovative materials used in biological and medical applications. They respond to magnetic field through the superparamagnetic behavior at room temperature. In this study, the MNPs were synthesized via the chemical co-precipitation method using various coating agents. Fatty acids, found naturally in the animal fats, can be used as a coating agent. Oleic acid and hexanoic acid were chosen as the surface modification agents to study the improvement in the suspension of MNPs in water and the magnetite properties. Suspension stability, particle size, and electrical conductivity of MNPs are critically affected by the modification process. The well-dispersed MNPs in water can be improved by the surface modification and the oleic acid coated MNPs possess excellent suspension stability over 1 week. The particle size of MNPs increases up to 40 nm using oleic acid coated MNPs. The electrical conductivity of the smallest particle size is 1.3x10-3 S/cm, which is 5 times higher than that of the largest particle, suggesting potential applications as a biomedical material under both of the electrical and magnetic fields.

  17. [Decorporation agents for internal radioactive contamination].

    Science.gov (United States)

    Ohmachi, Yasushi

    2015-01-01

    When radionuclides are accidentally ingested or inhaled, blood circulation or tissue/organ deposition of the radionuclides causes systemic or local radiation effects. In such cases, decorporation therapy is used to reduce the health risks due to their intake. Decorporation therapy includes reduction and/or inhibition of absorption from the gastrointestinal tract, isotopic dilution, and the use of diuretics, adsorbents, and chelating agents. For example, penicillamine is recommended as a chelating agent for copper contamination, and diethylene triamine pentaacetic acid is approved for the treatment of internal contamination with plutonium. During chelation therapy, the removal effect of the drugs should be monitored using a whole-body counter and/or bioassay. Some authorities, such as the National Council on Radiation Protection and Measurements and International Atomic Energy Agency, have reported recommended decorporation agents for each radionuclide. However, few drugs are approved by the US Food and Drug Administration, and many are off-label-use agents. Because many decontamination agents are drugs that have been available for a long time and have limited efficacy, the development of new, higher-efficacy drugs has been carried out mainly in the USA and France. In this article, in addition to an outline of decorporation agents for internal radioactive contamination, an outline of our research on decorporation agents for actinide (uranium and plutonium) contamination and for radio-cesium contamination is also presented. PMID:25832835

  18. The Influence of the Chelating Agent Nitrilotriacetic Acid on Promotion of Hydrodesulfurization Activity by Co in CoMo Catalysts Prepared on Al2O3, C, and ZrO2 Supports

    OpenAIRE

    Kaluža, L. (Luděk); Zdražil, M. (Miroslav); Gulková, D. (Daniela); Vít, Z. (Zdeněk)

    2013-01-01

    The chelating agent NTA systematically increased the promotion effect of Co in the sulfided catalysts in comparison to samples prepared without NTA from ammonium heptamolybdate and cobalt nitrate. The promotion effect was increased by the factor 1.13-1.58.

  19. Agent Development Toolkits

    CERN Document Server

    Singh, Aarti; Sharma, A K

    2011-01-01

    Development of agents as well as their wide usage requires good underlying infrastructure. Literature indicates scarcity of agent development tools in initial years of research which limited the exploitation of this beneficial technology. However, today a wide variety of tools are available, for developing robust infrastructure. This technical note provides a deep overview of such tools and contrasts features provided by them.

  20. Asimovian Adaptive Agents

    CERN Document Server

    Gordon, D F

    2011-01-01

    The goal of this research is to develop agents that are adaptive and predictable and timely. At first blush, these three requirements seem contradictory. For example, adaptation risks introducing undesirable side effects, thereby making agents' behavior less predictable. Furthermore, although formal verification can assist in ensuring behavioral predictability, it is known to be time-consuming. Our solution to the challenge of satisfying all three requirements is the following. Agents have finite-state automaton plans, which are adapted online via evolutionary learning (perturbation) operators. To ensure that critical behavioral constraints are always satisfied, agents' plans are first formally verified. They are then reverified after every adaptation. If reverification concludes that constraints are violated, the plans are repaired. The main objective of this paper is to improve the efficiency of reverification after learning, so that agents have a sufficiently rapid response time. We present two solutions: ...

  1. How do agents represent?

    Science.gov (United States)

    Ryan, Alex

    Representation is inherent to the concept of an agent, but its importance in complex systems has not yet been widely recognised. In this paper I introduce Peirce's theory of signs, which facilitates a definition of representation in general. In summary, representation means that for some agent, a model is used to stand in for another entity in a way that shapes the behaviour of the agent with respect to that entity. Representation in general is then related to the theories of representation that have developed within different disciplines. I compare theories of representation from metaphysics, military theory and systems theory. Additional complications arise in explaining the special case of mental representations, which is the focus of cognitive science. I consider the dominant theory of cognition — that the brain is a representational device — as well as the sceptical anti-representational response. Finally, I argue that representation distinguishes agents from non-representational objects: agents are objects capable of representation.

  2. Hyperthermia and chemotherapy agent

    International Nuclear Information System (INIS)

    The use of chemotherapeutic agents for the treatment of cancer dates back to the late 19th century, but the modern era of chemotherapy drugs was ushered in during the 1940's with the development of the polyfunctional alkylating agent. Since then, numerous classes of drugs have evolved and the combined use of antineoplastic agents with other treatment modalities such as radiation or heat, remains a large relatively unexplored area. This approach, combining local hyperthermia with chemotherapy agents affords a measure of targeting and selective toxicity not previously available for drugs. In this paper, the effects of adriamycin, bleomycin and cis-platinum are examined. The adjuvant use of heat may also reverse the resistance of hypoxic cells noted for some chemotherapy agents

  3. Preventing acute rejection, Epstein-Barr virus infection, and posttransplant lymphoproliferative disorders after kidney transplantation: Use of aciclovir and mycophenolate mofetil in a steroid-free immunosuppressive protocol

    DEFF Research Database (Denmark)

    Birkeland, S.A.; Andersen, H.K.; Hamilton-Dutoit, Stephen Jacques

    1999-01-01

    Background: A widely held view is that any increase in the potency of an immunosuppressive agent will lead to an increase in infection and malignancy, such as life-threatening Epstein-Barr virus (EBV) induced posttransplant lymphoproliferative disorders (PTLD), We tested this paradigm by studying......: (1) primary or reactivated EBV infection (PREBV) was correlated to acute rejection (treated with OKT3; P<0.00005) and to the incidence of PTLD (P=0.03; P=0.01, if Hodgkin's disease is included); (2) aciclovir protected against PREBV (P<0.00005) and (3) adding mofetil to the immunosuppressive protocol...... immunosuppression with mofetil protects against acute rejection. In combination with aciclovir, there is also a reduction in the number of PREBVs, apparently as a result of both direct viral prophylaxis and better rejection control, and in the incidence of EBV-induced PTLD Udgivelsesdato: 1999...

  4. Users, Bystanders and Agents

    DEFF Research Database (Denmark)

    Krummheuer, Antonia Lina

    2015-01-01

    Human-agent interaction (HAI), especially in the field of embodied conversational agents (ECA), is mainly construed as dyadic communication between a human user and a virtual agent. This is despite the fact that many application scenarios for future ECAs involve the presence of others. This paper...... the construction of the agent’s identity, and (3) how HAI, as a mediated interaction, is framed by an asymmetric participation framework. The paper concludes by suggesting various participation roles, which may inform development of ECAs....

  5. Agent-Based Optimization

    CERN Document Server

    Jędrzejowicz, Piotr; Kacprzyk, Janusz

    2013-01-01

    This volume presents a collection of original research works by leading specialists focusing on novel and promising approaches in which the multi-agent system paradigm is used to support, enhance or replace traditional approaches to solving difficult optimization problems. The editors have invited several well-known specialists to present their solutions, tools, and models falling under the common denominator of the agent-based optimization. The book consists of eight chapters covering examples of application of the multi-agent paradigm and respective customized tools to solve  difficult optimization problems arising in different areas such as machine learning, scheduling, transportation and, more generally, distributed and cooperative problem solving.

  6. ACETIC ACID AND A BUFFER

    DEFF Research Database (Denmark)

    2009-01-01

    The present invention relates to a composition comprising : a) 0.01-20% wt/wt acetic acid and b) a physiologically tolerable buffer capable of maintaining acetic acid at a pH in the range of 2-7; and use of such a composition as an antimicrobial agent.......The present invention relates to a composition comprising : a) 0.01-20% wt/wt acetic acid and b) a physiologically tolerable buffer capable of maintaining acetic acid at a pH in the range of 2-7; and use of such a composition as an antimicrobial agent....

  7. Acid Deposition Phenomena

    International Nuclear Information System (INIS)

    Acid deposition, commonly known as acid rain, occurs when emissions from the combustion of fossil fuels and other industrial processes undergo complex chemical reactions in the atmosphere and fall to the earth as wet deposition (rain, snow, cloud, fog) or dry deposition (dry particles, gas). Rain and snow are already naturally acidic, but are only considered problematic when less than a ph of 5.0 The main chemical precursors leading to acidic conditions are atmospheric concentrations of sulfur dioxide (SO2) and nitrogen oxides (NOx). When these two compounds react with water, oxygen, and sunlight in the atmosphere, the result is sulfuric (H2SO4) and nitric acids (HNO3), the primary agents of acid deposition which mainly produced from the combustion of fossil fuel and from petroleum refinery. Airborne chemicals can travel long distances from their sources and can therefore affect ecosystems over broad regional scales and in locations far from the sources of emissions. According to the concern of petroleum ministry with the environment and occupational health, in this paper we will discussed the acid deposition phenomena through the following: Types of acidic deposition and its components in the atmosphere Natural and man-made sources of compounds causing the acidic deposition. Chemical reactions causing the acidic deposition phenomenon in the atmosphere. Factors affecting level of acidic deposition in the atmosphere. Impact of acid deposition. Procedures for acidic deposition control in petroleum industry

  8. Agent Standards Project

    Data.gov (United States)

    National Aeronautics and Space Administration — The innovation of the work herein proposed is the development of standards for software autonomous agents. These standards are essential to achieve software...

  9. Programming Service Oriented Agents

    OpenAIRE

    Hirsch, Benjamin; Konnerth, Thomas; Burkhardt, Michael; Albayrak, Sahin

    2010-01-01

    This paper introduces a programming language for service-oriented agents. JADL++ combines the ease of use of scripting-languages with a state-of-the-art service oriented approach which allows the seamless integration of web-services. Furthermore, the language includes OWL-based ontologies for semantic descriptions of data and services, thus allowing agents to make intelligent decisions about service calls.

  10. 米根霉发酵产富马酸的最适替代中和剂及pH调控策略研究%Search for Optimum Substitutive Neutralizing Agent and pH Control Strategy in Fumaric Acid Fermentation by Rhizopus oryzae

    Institute of Scientific and Technical Information of China (English)

    陈晨; 邰超; 李霜

    2013-01-01

    Four different neutralizing agents ( CaCO3, Na2CO3, NH3 · H2O, NaOH) were chosen to examine the effects of neutralizing agents on fumaric acid fermentation by Rhizopus oryzae ME-F12 which is the mutant of R. oryzae ATCC 20344. It was found that fumaric acid yield and productivity in the fermentation using Na2CO3 as neutralizing agent were the closest to which in the traditional CaCO3 case. Then the effects of different pH values (3.5, 4.5, 5. 5, and 6. 5) on fumaric acid fermentation using Na2CO3 as neutralizing agent were investigated. Based on the analysis of three kinetic parameters, a two-stage pH control strategy, aimed at achieving high concentration, high yield and high productivity of fumaric acid simultaneously, was proposed. pH was controlled at 5.5 at the first 24 h, and then switched to 4. 5 till the end of the fermentation. Finally, the maximum concentration of fumaric acid reached 40. 5 g/L with the yield of 0. 55 g/g and the productivity of 0. 61 g/L/h, which were 8.3% , 10.0% and 17. 3% higher than the best result of constant pH control process. Its productivity was even 3.4% higher than which in CaCO3 case. With the internal advantages of reducing power consumption and simplifying downstream processing, using Na2CO3 as neutralizing agent under two-stage pH control strategy successfully take place of CaCO3.%针对米根霉发酵产富马酸使用的不同中和剂(CaCO3,Na2CO3,NH3·H2O,NaOH)进行了研究,结果表明发酵过程中使用Na2CO3作为中和剂时富马酸产率和生产强度最接近传统中和剂CaCO3.此后考察了不同pH值(3.5,4.5,5.5和6.5)对Na2CO3作为中和剂的富马酸发酵过程的影响.基于对3个动力学参数的分析,提出了一个旨在同时获得富马酸高产物浓度、高产率和高生产强度的双阶段pH调控策略,在初始的24 h内pH控制在5.5,然后将pH调到4.5直至发酵结束.最终富马酸的终浓度达到40.5 g/L,产率为0.55 g/g,生产强度为0.61 g/L/h,比恒定pH时

  11. Agent amplified communication

    Energy Technology Data Exchange (ETDEWEB)

    Kautz, H.; Selman, B.; Milewski, A. [AT& T Laboratories, Murray Hill, NJ (United States)

    1996-12-31

    We propose an agent-based framework for assisting and simplifying person-to-person communication for information gathering tasks. As an example, we focus on locating experts for any specified topic. In our approach, the informal person-to-person networks that exist within an organization are used to {open_quotes}referral chain{close_quotes} requests for expertise. User-agents help automate this process. The agents generate referrals by analyzing records of e-mail communication patterns. Simulation results show that the higher responsiveness of an agent-based system can be effectively traded for the higher accuracy of a completely manual approach. Furthermore, preliminary experience with a group of users on a prototype system has shown that useful automatic referrals can be found in practice. Our experience with actual users has also shown that privacy concerns are central to the successful deployment of personal agents: an advanced agent-based system will therefore need to reason about issues involving trust and authority.

  12. Bioprotective agents in safety control

    Directory of Open Access Journals (Sweden)

    Dimitrijević-Branković Suzana I.

    2003-01-01

    Full Text Available Food poisoning is the one of the main health hazards even today. More than 200 known diseases are transmitted through food. The causes of foodborne illness include viruses, bacteria, parasites, toxins, metals, and prions and the symptoms of foodborne illness range from mild gastroenteritis to life-threatening neurological, hepatic and renal syndromes.The prevention of food poisonings represents very serious task for food manufacturers. Beside food control according to the concept "from the farm to the table" there is increased need for the development of new technology for longer shelf lifes of food. Food fermented by lactic acid bacteria (LAB and traditionally considered to be safe. There are many substances produced by LAB that affect the shelf life of fermented food, by active suppression of poisoning microorganisms growth. Because of that, the LAB is recently considered as bioprotective agents that have important role in food safety.

  13. Host modulation by therapeutic agents

    Directory of Open Access Journals (Sweden)

    Sugumari Elavarasu

    2012-01-01

    Full Text Available Periodontal disease susceptible group present advanced periodontal breakdown even though they achieve a high standard of oral hygiene. Various destructive enzymes and inflammatory mediators are involved in destruction. These are elevated in case of periodontal destruction. Host modulation aims at bringing these enzymes and mediators to normal level. Doxycycline, nonsteroidal anti-inflammatory drugs (NSAIDs, bisphosphonates, nitrous oxide (NO synthase inhibitors, recombinant human interleukin-11 (rhIL-11, omega-3 fatty acid, mouse anti-human interleukin-6 receptor antibody (MRA, mitogen-activated protein kinase (MAPK inhibitors, nuclear factor-kappa B (NF-kb inhibitors, osteoprotegerin, and tumor necrosis factor antagonist (TNF-α are some of the therapeutic agents that have host modulation properties.

  14. Nanometer TiO2 Modified Polyacrylic Copolymer Sizing Agent

    Institute of Scientific and Technical Information of China (English)

    2007-01-01

    A series of new-type nanometer TiO2 modified polyacrylic copolymer sizing agent were synthesized from acrylic acid, ethyl acrylate, nanometer TiO2, oleic acid etc.by orthogonal design method. Results of the studies show that the synthetic method used in this paper was a new way and had never been found in the synthesis of acrylate sizing agent, and that the properties of those new-type size-agent were be improved, which had potential for substituting PVA (polyvinyl alcohol) sizing agent. The technology for solving the problem of nano-scale powder agglomeration and dispersion were also studied. The transmission electron microscope (TEM) observation showed that nano-TiO2 had good dispersion and stability in aqueous solution and in sizing agent solution.

  15. Positively charged co-polymers for use as antimicrobial agents

    DEFF Research Database (Denmark)

    2016-01-01

    The present invention provides a positively charged co-polymer for use as an antimicrobial agent, wherein said positively charged co-polymer is composed of amino acids and/or derivatives thereof and wherein at least 75 molar percent of said amino acids are selected from the group consisting of...

  16. Ethylenediaminetetraacetic acid in endodontics

    OpenAIRE

    Mohammadi, Zahed; Shalavi, Sousan; Jafarzadeh, Hamid

    2013-01-01

    Ethylenediaminetetraacetic acid (EDTA) is a chelating agent can bind to metals via four carboxylate and two amine groups. It is a polyamino carboxylic acid and a colorless, water-soluble solid, which is widely used to dissolve lime scale. It is produced as several salts, notably disodium EDTA and calcium disodium EDTA. EDTA reacts with the calcium ions in dentine and forms soluble calcium chelates. A review of the literature and a discussion of the different indications and considerations for...

  17. TOWARDS A RATIONAL DESIGN OF RESOLVING AGENTS .4. CRYSTAL PACKING ANALYSES AND MOLECULAR MECHANICS CALCULATIONS FOR 5 PAIRS OF DIASTEREOMERIC SALTS OF EPHEDRINE AND A CYCLIC PHOSPHORIC-ACID

    NARCIS (Netherlands)

    LEUSEN, FJJ; SLOT, HJB; NOORDIK, JH; VANDERHAEST, AD; WYNBERG, H; BRUGGINK, A

    1992-01-01

    Detailed structural studies of five pairs of diastereomeric salts of ephedrine and halogen-substituted chiral cyclic phosphoric acids indicate a correlation between the efficiency of the resolution process and the lattice energy difference between the salts of a diastereomeric pair. Attempts to mode

  18. IV. Study of the stability of 14C-labelled coumaphos in the presence of sediment, an acidic buffer and a bacteriostatic agent in model dipping vats under outdoor conditions

    International Nuclear Information System (INIS)

    The effect of the addition of sediment, a buffering agent (superphosphate fertilizer) and a bacteriostat (copper sulphate) on the stability of 14C-labelled coumaphos in suspension in model dipping vats was studied for a period of 180 days under outdoor conditions. At the end of this period the highest proportion of the initial radioactivity (36%) was in the vats containing coumaphos suspension with no additives and the lowest (10%) in the vats in which the bacteriostat and sediment were added to coumaphos suspension. Recovery was lowered in all vats to which sediment or the bacteriostat had been added. In the presence of sediment or the bacteriostat addition of the buffering agent did not have any affect on the levels of radioactivity after 180 days. Thus, the addition of superphosphate to coumaphos suspension containing bacteriostat reduced the radioactivity from 26% to 23% of the initial amount. The radioactivity level was 10% in the suspension to which sediment had been added and 12 % to which both sediment and superphosphate were added. (author)

  19. Degradation products of benzyldibutylamine as extraction agent

    International Nuclear Information System (INIS)

    The composition of the degradation products of benzyldibutylamine (BDBuN) and benzene radiolysis in the presence of nitric acid and lanthanide nitrates was identified by means of mass, NMR and infrared spectra, elementary analysis and gas liquid chromatography. The change in the extraction capacity of this agent and its solutions in aromatic hydrocarbon solvents in the extraction of Eu/III/ and Am/III/ was investigated in dependence on the absorbed dose of the ionising radiation. (author)

  20. Degradation products of benzyldibutylamine as extracton agent

    Science.gov (United States)

    Mirchi, R.; Jedinakova, V.

    The composition of the degradation products of benzyldibutylamine (BDBuN) and benzene radiolysis in the presence of nitric acid and lanthanide nitrates was identified by means of mass, NMR and infrared spectra, elementary analysis and gas liquid chromatography. The change in the extraction capacity of this agent and its solutions in aromatic hydrocarbon solvents in the extraction of Eu/III/ and Am/III/ was investigated in dependence on the absorbed dose of the ionising radiation.

  1. EDTA: the chelating agent under environmental scrutiny

    OpenAIRE

    Claudia Oviedo; Jaime Rodríguez

    2003-01-01

    The chelating agent EDTA (ethylenediaminetetraacetic acid) is a compound of massive use world wide with household and industrial applications, being one of the anthropogenic compounds with highest concentrations in inland European waters. In this review, the applications of EDTA and its behavior once it has been released into the environment are described. At a laboratory scale, degradation of EDTA has been achieved; however, in natural environments studies detect poor biodegradability. It is...

  2. Agent Oriented Programming进展%Advances in Agent Oriented Programming

    Institute of Scientific and Technical Information of China (English)

    王一川; 石纯一

    2002-01-01

    Agent-oriented programming (AOP) is a framework to develop agents, and it aims to link the gap betweentheory and practical in agent research. The core of an AOP framework is its language and semantics. In this paper,we propose the necessary properties which agents should have, and then give a summary and analysis about differentAOP languages based on these properties.

  3. Metal-Based Antibacterial and Antifungal Agents: Synthesis, Characterization, and In Vitro Biological Evaluation of Co(II), Cu(II), Ni(II), and Zn(II) Complexes With Amino Acid-Derived Compounds

    OpenAIRE

    Zahid H. Chohan; Arif, M.; Akhtar, Muhammad A.; Supuran, Claudiu T.

    2006-01-01

    A series of antibacterial and antifungal amino acid-derived compounds and their cobalt(II), copper(II), nickel(II), and zinc(II) metal complexes have been synthesized and characterized by their elemental analyses, molar conductances, magnetic moments, and IR, and electronic spectral measurements. Ligands (L1)−(L5) were derived by condensation of β-diketones with glycine, phenylalanine, valine, and histidine and act as bidentate towards metal ions (cobalt, copper, nickel, and zinc) via the azo...

  4. Agents unleashed a public domain look at agent technology

    CERN Document Server

    Wayner, Peter

    1995-01-01

    Agents Unleashed: A Public Domain Look at Agent Technology covers details of building a secure agent realm. The book discusses the technology for creating seamlessly integrated networks that allow programs to move from machine to machine without leaving a trail of havoc; as well as the technical details of how an agent will move through the network, prove its identity, and execute its code without endangering the host. The text also describes the organization of the host's work processing an agent; error messages, bad agent expulsion, and errors in XLISP-agents; and the simulators of errors, f

  5. Fatty acid as structure directing agent for controlled secondary growth of CoFe2O4 nanoparticles to achieve mesoscale assemblies: A facile approach for developing hierarchical structures

    Science.gov (United States)

    Saikia, K.; Kaushik, S. D.; Sen, D.; Mazumder, S.; Deb, P.

    2016-08-01

    Mesoscale hierarchical assemblies have emerged out as a new class of structures between fine dimension nanoparticles and bulk structures, having distinctly different physical properties from either side. Controlling the self-assembly process of primary nanoparticles and subsequent secondary growth mechanism is the key aspect for achieving such ordered structures. In this work, we introduce a new insight on achieving hierarchical assemblies of CoFe2O4 nanoparticles based on the temporal stability of the primary nanoparticles, where, the growth and stability of the primary particles are controlled by using oleic acid. It is found that the developed particles, at a critical concentration of oleic acid, prefer a secondary growth process, rather than promoting their individual growth. Domination of the attractive hydrophobic interaction over steric repulsion among the primary particles at this critical concentration of oleic acid is found to be the key factor for the initial aggregation of the primary particles, which eventually leads to the formation of spherical hierarchical assemblies via oriented attachment. It is also realized that the extremely well or poor stability conditions of the primary particles do not allow this secondary growth process. Estimated values of Co2+ distribution factor show that the cation distribution factor of CoFe2O4 system is not affected by the nature of dominant growth processes, when these are controlled. Interestingly, magnetic measurements reflect the stronger interparticle interaction in the hierarchical system and high magnetic moment values at low magnetic field.

  6. El agente encubierto

    OpenAIRE

    Anaya Marcos, María del Carmen

    2015-01-01

    [ES] El trabajo versa sobre la figura del agente encubierto. Debemos enmarcar tal medida de investigación dentro del ámbito de la criminalidad organizada. Actualmente, estamos asistiendo a una proliferación de la delincuencia organizada. La sociedad ha evolucionado, y con ella la delincuencia. Fruto de tal evolución fue necesario incluir en nuestra Ley de Enjuiciamiento Criminal medidas extraordinarias de investigación, y una de ellas es el agente encubierto. Se trata de una medida muy polémi...

  7. The PLS agent : agent behavior validation by partial least squares

    OpenAIRE

    Lorscheid, Iris; Meyer, Matthias; Pakur, Sandra; Ringle, Christian

    2014-01-01

    Agent-based modeling is widely applied in the social sciences. However, the validation of agent behavior is challenging and identified as one of the shortcomings in the field. Methods are required to establish empirical links and support the implementation of valid agent models. This paper contributes to this, by introducing the PLS agent concept. This approach shows a way to transfer results about causalities and decision criteria from empirical surveys into an agent-based decision model, th...

  8. Trading Agents for Roaming Users

    OpenAIRE

    Boman, Magnus; Bylund, Markus; Espinoza, Fredrik; Danielson, Mats; Lyback, David

    2002-01-01

    Some roaming users need services to manipulate autonomous processes. Trading agents running on agent trade servers are used as a case in point. We present a solution that provides the agent owners with means to upkeeping their desktop environment, and maintaining their agent trade server processes, via a briefcase service.

  9. Software Agent Techniques in Design

    DEFF Research Database (Denmark)

    Hartvig, Susanne C

    1998-01-01

    This paper briefly presents studies of software agent techniques and outline aspects of these which can be applied in design agents in integrated civil engineering design environments.......This paper briefly presents studies of software agent techniques and outline aspects of these which can be applied in design agents in integrated civil engineering design environments....

  10. 13 CFR 107.1620 - Functions of agents, including Central Registration Agent, Selling Agent and Fiscal Agent.

    Science.gov (United States)

    2010-01-01

    ... 13 Business Credit and Assistance 1 2010-01-01 2010-01-01 false Functions of agents, including Central Registration Agent, Selling Agent and Fiscal Agent. 107.1620 Section 107.1620 Business Credit and Assistance SMALL BUSINESS ADMINISTRATION SMALL BUSINESS INVESTMENT COMPANIES SBA Financial Assistance...

  11. Programming multi-agent systems

    NARCIS (Netherlands)

    Dastani, Mehdi

    2015-01-01

    With the significant advances in the area of autonomous agents and multi-agent systems in the last decade, promising technologies for the development and engineering of multi-agent systems have emerged. The result is a variety of agent-oriented programming languages, development frameworks, executio

  12. SECOND BUYING AGENT

    CERN Multimedia

    SPL - SERVICES ACHATS

    2000-01-01

    Last year the buying agent LOGITRADE started operations on the CERN site, processing purchasing requests for well-defined families of products up to a certain value. It was planned from the outset that a second buying agent would be brought in to handle the remaining product families. So, according to that plan, the company CHARLES KENDALL will be commencing operations at CERN on 8 May 2000 in Building 73, 1st floor, offices 31 and 35 (phone and fax numbers to be announced).Each buying agent will have its own specific list of product families and will handle purchasing requests up to 10'000 CHF.Whenever possible they will provide the requested supplies at a price (including the cost of their own services) which must be equivalent to or lower than the price mentioned on the purchasing request, changing the supplier if necessary. If a lower price cannot be obtained, agents will provide the necessary administrative support free of charge.To ensure that all orders are processed in the best possible conditions, us...

  13. Developing Enculturated Agents

    DEFF Research Database (Denmark)

    Rehm, Matthias

    Embodied Conversational Agents (ECAs) are complex multimodal systems with rich verbal and nonverbal repertoires. There human-like appearance raises severe expectations regarding natural communicative behaviors on the side of the user. But what is regarded as “natural” is to a large degree dependent...

  14. Biomimetic Emotional Learning Agents

    OpenAIRE

    Kenyon, Samuel H.

    2005-01-01

    This extended abstract proposes a type of AI agent comprised of: an autonomous real-time control system, low-level emotional learning (including a simple knowledge base that links homeostatic/innate drives to sensory perception states), and a novel sliding-priority drive motivation mechanism. Learning occurs in both phylogenetic and ontogenetic training.

  15. Agents of Change

    DEFF Research Database (Denmark)

    Hansen, Jens Aage; Lehmann, Martin

    2004-01-01

    at large, it emphasises universities as key change agents and providers in new learning, including tools such as project based and problem oriented learning (PBL) as well as information and communication technology (ICT); as providers of competent and motivated graduates to fill key positions in society...

  16. The need for agents

    DEFF Research Database (Denmark)

    Abolfazlian, Ali Reza Kian

    1996-01-01

    I denne artikel arbejder vi med begrebet Intelligent Software Agents (ISAs), som autonomous, social, reactive, proactive og subservient computer systemer. Baseret på socialt psykologiske argumenter viser jeg endvidere, hvordan både den menneskelige natur og det teknologiske stadium, som mennesket...

  17. Build Autonomic Agents with ABLE

    Institute of Scientific and Technical Information of China (English)

    吴吉义

    2007-01-01

    The IBM Agent Building and Learning Environment(ABLE) provides a lightweight Java~(TM) agent frame- work,a comprehensive JavaBeansTM library of intelligent software components,a set of development and test tools, and an agent platform.After the introduction to ABLE,classes and interfaces in the ABLE agent framework were put forward.At last an autonomic agent that is an ABLE-based architecture for incrementally building autonomic systems was discussed.

  18. 21 CFR 184.1009 - Adipic acid.

    Science.gov (United States)

    2010-04-01

    ... also known as 1,4-butanedicarboxylic acid or hexane-dioic acid. It is prepared by nitric acid oxidation... ethanol. The melting range of the ester is 153° to 154 °C. (c) The ingredient is used as a flavoring agent as defined in § 170.3(o)(12) of this chapter; leavening agent as defined in § 170.3(o)(17) of...

  19. Treatment of acid mine wastewaters

    International Nuclear Information System (INIS)

    Acid mine drainage often results from the oxidation sulfide minerals to form sulfuric acid. As a consequence, high concentrations of metals in the both the suspended and dissolved state result from the low pH water. This paper discusses several of the more common treatment methods for acid mine drainage including the use of chemical precipitation agents, pH correction agents, filtration methods, and biodegradation methods. Advanced treatment technologies are also briefly described and include microfiltration, reverse osmosis, ion exchange, and electrodialysis

  20. Microwave-assisted digestion using nitric acid for heavy metals and sulfated ash testing in active pharmaceutical ingredients.

    Science.gov (United States)

    Pluhácek, T; Hanzal, J; Hendrych, J; Milde, D

    2016-04-01

    The monitoring of inorganic impurities in active pharmaceutical ingredients plays a crucial role in the quality control of the pharmaceutical production. The heavy metals and residue on ignition/sulfated ash methods employing microwave-assisted digestion with concentrated nitric acid have been demonstrated as alternatives to inappropriate compendial methods recommended in United States Pharmacopoeia (USP) and European Pharmacopoeia (Ph. Eur.). The recoveries using the heavy metals method ranged between 89% and 122% for nearly all USP and Ph. Eur. restricted elements as well as the recoveries of sodium sulfate spikes were around 100% in all tested matrices. The proposed microwave-assisted digestion method allowed simultaneous decomposition of 15 different active pharmaceutical ingredients with sample weigh up to 1 g. The heavy metals and sulfated ash procedures were successfully applied to the determination of heavy metals and residue on ignition/sulfated ash content in mycophenolate mofetil, nicergoline and silymarin. PMID:27209695

  1. Evaluation of different cleaning agents used for cleaning ultra tiltration membranes fouled by surface water

    OpenAIRE

    Zondervan, Edwin; Roffel, Brian

    2007-01-01

    This paper reviews the published literature on potential membrane fouling components, available cleaning agents and possible interactions between cleaning agents and fouling components. It also lists the cleaning models available in the literature, and evaluates the advantages and disadvantages of these models. Based on this outcome, a new cleaning model is proposed to capture cleaning dynamics for 10 different cleaning agents, varying from acidic, alkali and oxidizing to sequestering agents ...

  2. New Regulation Agent on Conjugated Linoleic Acid in Milk-Compositae%乳中共轭亚油酸生成的新型调控剂——菊科植物

    Institute of Scientific and Technical Information of China (English)

    王丽芳; 卢德勋; 丁国和; 马燕芬

    2011-01-01

    共轭亚油酸(CLA)是一组含有共轭双键的亚油酸(linoleic acid)的几何异构体和位置异构体的总称。目前有研究报道,菊科植物及其提取物能增加乳中CLA的含量。主要综述了CLA的营养调控方法及菊科植物增加CLA含量的研究进展。%The conjugated linoleic acid(CLA) was a general name of a group of geometric isomer and positional isomer that contained linoleic acid with conjugated double bond.At present,researches showed that the compositae and its extract could increase the CLA content in milk.The nutritional regulation method of CLA and increasing CLA content by compositae in the previous research reports were reviewed in this paper.

  3. Design and synthesis of isoniazide mimetic conjugated with DTPA, potential ligand of novel radiopharmaceutical and contrast agent for medical imaging, bis (amide) of diethylenetriaminepentaacetic acid: DTPA-Bis(INH)

    International Nuclear Information System (INIS)

    The structure of isonicotinic acid hydrazide (INH) was coupled to diethylenetriaminepentaacetic acid (DTPA) via amide linkage. The overall yield of three steps synthesis starting from DTPA is above 80%. In particular, complexation of DTPA moiety with 99mTc showed excellent results as the metallopharmaceutical for medical imaging. The main objective of the present research was to develop a novel INH derivative based on DTPA, which forms stable complexes with most of the lanthanides and transition metals in the periodic table. A second objective was to introduce a chelating group without compromising the biological activity of the anti-infective drug for the diagnosis of infection using nuclear medicine. The DTPA-Bis(INH) was synthesized in high yield using a simple synthetic procedure and was characterized using mass spectroscopy in ESI positive mode ([M+H+] was found to be 632.2). Moreover, the complex with the DTPA-Bis(INH) is reflected in increased kinetic ability of the stabilized 99mTc complex compared with the unmodified INH. The complex was successfully labelled with the 99mTc radionuclide with more than 95% labelling efficiency. Radiochemical purity was ascertained chromatographically (ITLC and C18 RP chromatography) using different solvent systems. Blood kinetics in rabbits and biodistribution in mice was studied. Blood kinetics showed rapid first pass clearance with a biological half-life, t1/2 (F), of 11 min. The ability of DTPA-Bis(INH) to target the infection site in vivo was assessed in gamma scintigraphic studies of normal rabbit and a rabbit with induced infections. From the present work it can be concluded that the radiolabelled DTPABis( INH) accumulates at the site of infection. (author)

  4. Immunoregulatory profiles in liver transplant recipients on different immunosuppressive agents

    OpenAIRE

    Levitsky, Josh; Miller, Joshua; Wang, Edward; Rosen, Anne; Flaa, Cathy; Abecassis, Michael; Mathew, James; Tambur, Anat

    2009-01-01

    We compared peripheral blood immunophenotyping in 31 adult liver transplant recipients on differing long-term immunosuppressive (IS) monotherapy with and without peri-transplantation alemtuzumab (AL) induction. All patients had been stable on monotherapy with either sirolimus (SRL) (n = 10) or without SRL (tacrolimus (TAC) (n = 10), mycophenolate mofetil (MMF) (n = 11)) for more than 6 months. Five-color flow cytometry for putative “regulatory” T and dendritic cells as well as serum assays fo...

  5. Actions and Agents

    OpenAIRE

    Alonso, E.

    2014-01-01

    In this chapter the notion of agency in AI is presented..It has been argued that in order to behave rationally in prevalent software applications artificial entities would have to be autonomous and adaptive. Besides, rather than working with single, isolated systems the new trend in AI would need to focus on inherently social entities in the form of multi-agent systems. The chapter begins by introducing the notion of action in traditional AI systems, deliberative and reactive. Next, the i...

  6. Towards Soft Computing Agents

    Czech Academy of Sciences Publication Activity Database

    Neruda, Roman; Krušina, Pavel; Petrová, Zuzana

    2000-01-01

    Roč. 10, č. 5 (2000), s. 859-868. ISSN 1210-0552. [SOFSEM 2000 Workshop on Soft Computing. Milovy, 27.11.2000-28.11.2000] R&D Projects: GA ČR GA201/00/1489; GA ČR GA201/99/P057 Institutional research plan: AV0Z1030915 Keywords : hybrid systems * intelligent agents Subject RIV: BA - General Mathematics

  7. Sunscreening Agents: A Review

    OpenAIRE

    Latha, M. S.; Martis, Jacintha; Shobha, V; Sham Shinde, Rutuja; Bangera, Sudhakar; Krishnankutty, Binny; Bellary, Shantala; Varughese, Sunoj; Rao, Prabhakar; B R Naveen Kumar

    2013-01-01

    The increasing incidence of skin cancers and photodamaging effects caused by ultraviolet radiation has increased the use of sunscreening agents, which have shown beneficial effects in reducing the symptoms and reoccurrence of these problems. Many sunscreen compounds are in use, but their safety and efficacy are still in question. Efficacy is measured through indices, such as sun protection factor, persistent pigment darkening protection factor, and COLIPA guidelines. The United States Food an...

  8. Perioperative allergy: uncommon agents.

    Science.gov (United States)

    Caimmi, S; Caimmi, D; Cardinale, F; Indinnimeo, L; Crisafulli, G; Peroni, D G; Marseglia, G L

    2011-01-01

    Anesthesia may often be considered as a high-risk procedure and anaphylaxis remains a major cause of concern for anesthetists who routinely administer many potentially allergenic agents. Neuromuscular blocking agents, latex and antibiotics are the substances involved in most of the reported reactions. Besides these three agents, a wide variety of substances may cause an anaphylactic reaction during anesthesia. Basically all the administered drugs or substances may be potential causes of anaphylaxis. Among them, those reported the most in literature include hypnotics, opioids, local anesthetics, colloids, dye, Non-Steroidal Anti-Inflammatory Drugs (NSAIDs), Iodinated Contrast Media (ICM), antiseptics, aprotinin, ethylene oxyde and formaldehyde, and protamine and heparins. No premedication can effectively prevent an allergic reaction and a systematic preoperative screening is not justified for all patients; nevertheless, an allergy specialist should evaluate those patients with a history of anesthesia-related allergy. Patients must be fully informed of investigation results, and advised to provide a detailed report prior to future anesthesia. PMID:22014927

  9. Advanced scale conditioning agents

    International Nuclear Information System (INIS)

    A technical description of Advanced Scale Conditioning Agents (ASCA) technology was published in the May-June 2003 edition of the Nuclear Plant Journal. That article described the development of programs of advanced scale conditioning agents and specific types to maintain the secondary side of steam generators within a pressurized water reactor free of deposited corrosion products and corrosion-inducing contaminants to ensure their long-term operation. This article describes the first two plant applications of advanced scale conditioning agents implemented at Southern Nuclear Operating Company's Vogtle Units 1 and 2 during their 2002 scheduled outages to minimize tube degradation and maintain full power operation using the most effective techniques while minimizing outage costs. The goal was to remove three to four fuel cycles of deposits from each steam generator so that after future chemical cleaning activities, ASCAs could be used to maintain the cleanliness of the steam generators without the need for additional chemical cleaning efforts. The goal was achieved as well as several other benefits that resulted in cost savings to the plant

  10. SAM : Semantic Agent Model for SWRL rule-based agents

    OpenAIRE

    Subercaze, Julien; Maret, Pierre

    2010-01-01

    International audience SemanticWeb technologies are part of multi-agent engineering, especially regarding knowledge base support. Recent advances in the field of logic for the semantic web enable a new range of applications. Among them, programming agents based on semantic rules is a promising field. In this paper we present a semantic agent model that allows SWRL programming of agents. Our approach, based on the extended finite state machine concept, results in a three layers architecture...

  11. Metal-Based Antibacterial and Antifungal Agents: Synthesis, Characterization, and In Vitro Biological Evaluation of Co(II, Cu(II, Ni(II, and Zn(II Complexes with Amino Acid-Derived Compounds

    Directory of Open Access Journals (Sweden)

    Zahid H. Chohan

    2006-01-01

    Full Text Available A series of antibacterial and antifungal amino acid-derived compounds and their cobalt(II, copper(II, nickel(II, and zinc(II metal complexes have been synthesized and characterized by their elemental analyses, molar conductances, magnetic moments, and IR, and electronic spectral measurements. Ligands (L1–(L5 were derived by condensation of β-diketones with glycine, phenylalanine, valine, and histidine and act as bidentate towards metal ions (cobalt, copper, nickel, and zinc via the azomethine-N and deprotonated-O of the respective amino acid. The stoichiometric reaction between the metal(II ion and synthesized ligands in molar ratio of M: L (1: 1 resulted in the formation of the metal complexes of type [M(L(H2O4]Cl (where M = Co(II, Cu(II, and Zn(II and of M: L (1: 2 of type [M(L2(H2O2] (where M = Co(II, Cu(II, Ni(II, and Zn(II. The magnetic moment data suggested for the complexes to have an octahedral geometry around the central metal atom. The electronic spectral data also supported the same octahedral geometry of the complexes. Elemental analyses and NMR spectral data of the ligands and their metal(II complexes agree with their proposed structures. The synthesized ligands, along with their metal(II complexes, were screened for their in vitro antibacterial activity against four Gram-negative (Escherichia coli, Shigella flexeneri, Pseudomonas aeruginosa, and Salmonella typhi and two Gram-positive (Bacillus subtilis and Staphylococcus aureus bacterial strains and for in vitro antifungal activity against Trichophyton longifusus, Candida albicans, Aspergillus flavus, Microsporum canis, Fusarium solani, and Candida glaberata. The results of these studies show the metal(II complexes to be more antibacterial/antifungal against one or more species as compared to the uncomplexed ligands. The brine shrimp bioassay was also carried out to study their in vitro cytotoxic properties. Five compounds, (3, (7, (10, (11, and (22, displayed potent cytotoxic

  12. Metal-Based Antibacterial and Antifungal Agents: Synthesis, Characterization, and In Vitro Biological Evaluation of Co(II), Cu(II), Ni(II), and Zn(II) Complexes With Amino Acid-Derived Compounds.

    Science.gov (United States)

    Chohan, Zahid H; Arif, M; Akhtar, Muhammad A; Supuran, Claudiu T

    2006-01-01

    A series of antibacterial and antifungal amino acid-derived compounds and their cobalt(II), copper(II), nickel(II), and zinc(II) metal complexes have been synthesized and characterized by their elemental analyses, molar conductances, magnetic moments, and IR, and electronic spectral measurements. Ligands (L(1))-(L(5)) were derived by condensation of beta-diketones with glycine, phenylalanine, valine, and histidine and act as bidentate towards metal ions (cobalt, copper, nickel, and zinc) via the azomethine-N and deprotonated-O of the respective amino acid. The stoichiometric reaction between the metal(II) ion and synthesized ligands in molar ratio of M : L (1 : 1) resulted in the formation of the metal complexes of type [M(L)(H(2)O)(4)]Cl (where M = Co(II), Cu(II), and Zn(II)) and of M : L (1 : 2) of type [M(L)(2)(H(2)O)(2)] (where M = Co(II), Cu(II), Ni(II), and Zn(II)). The magnetic moment data suggested for the complexes to have an octahedral geometry around the central metal atom. The electronic spectral data also supported the same octahedral geometry of the complexes. Elemental analyses and NMR spectral data of the ligands and their metal(II) complexes agree with their proposed structures. The synthesized ligands, along with their metal(II) complexes, were screened for their in vitro antibacterial activity against four Gram-negative (Escherichia coli, Shigella flexeneri, Pseudomonas aeruginosa, and Salmonella typhi) and two Gram-positive (Bacillus subtilis and Staphylococcus aureus) bacterial strains and for in vitro antifungal activity against Trichophyton longifusus, Candida albicans, Aspergillus flavus, Microsporum canis, Fusarium solani, and Candida glaberata. The results of these studies show the metal(II) complexes to be more antibacterial/antifungal against one or more species as compared to the uncomplexed ligands. The brine shrimp bioassay was also carried out to study their in vitro cytotoxic properties. Five compounds, (3), (7), (10), (11), and (22

  13. Design and synthesis of isoniazide mimetic conjugated with DTPA, potential ligand of novel radiopharmaceutical and contrast agent for medical imaging, Bis (amide) of diethyelene triaminepentaacetic acid: DTPA-Bis(INH)

    International Nuclear Information System (INIS)

    The structure of isonicotinic acid hydrazide was coupled to diethylenetriaminepentaacetic acid (DTPA) via amide linkage. The Overall yield of three steps synthesis starting from DTPA is above 80%. The new ligand binds with infection site through specific interaction with gene iniA, iniB and iniC under pathological conditions. In particular, complexation of DTPA moiety with 99mTc and Gd+III showed excellent results as metallopharmaceutical for medical imaging. Primary object of the present invention is to propose a novel INH derivative based on DTPA, which form stable complexes with most of lanthanides and transition metals in periodic table. Another object of the present invention is to introduce a chelating group without compromising its biological activity for early diagnosis of infection using nuclear medicine and MR techniques. The DTPA-Bis(INH) was synthesized in high yield using simple synthetic procedure. Radiochemical purity was ascertained chromatographically using different solvent system. Blood kinetics in rabbits and biodistribution in mice was studied. The ability of DTPA-Bis(INH) to target infection site in vivo was assessed in gamma scintigraphic studies of normal rabbit and a rabbit with induced tuberculosis. The DTPA-Bis(INH) was characterized by Mass spectroscopy in ESI positive mode, M+H+ was found to be 632.2.The complex was successfully labeled with 99mTc radionuclide with more than 95% labeling efficiency.It was found stable up to 24h. Blood kinetics showed rapid first pass clearance with biological half life t1/2 (F) = 11 min. Imaging of a normal rabbit and a rabbit with induced tuberculosis was carried out. An appreciable activity was visualized in liver and kidneys. In diseased rabbit similar pattern was observed with the accumulation of activity at the tubercular site at 24 h post injection. Biodistribution revealed major accumulation in liver 6.30±0.58%ID/g at 1 h and 6.25±0.11 at 4h and in kidneys 7.65±0.52%ID/g at 1h and 6.70±0

  14. De novo design, synthesis and spectroscopic characterization of chiral benzimidazole-derived amino acid Zn(II) complexes: Development of tryptophan-derived specific hydrolytic DNA artificial nuclease agent

    Science.gov (United States)

    Parveen, Shazia; Arjmand, Farukh

    2012-01-01

    Novel ternary dizinc(II) complexes 1- 3, derived from 1,2-bis(1H-benzimidazol-2-yl)ethane-1,2-diol and L-form of amino acids (viz., tryptophan, leucine and valine) were synthesized and characterized by spectroscopic (IR, 1H NMR, UV-vis, ESI-MS) and other analytical methods. To evaluate the biological preference of chiral drugs for inherently chiral target DNA, interaction of 1- 3 with calf thymus DNA in Tris-HCl buffer was studied by various biophysical techniques which reveal that all these complexes bind to CT DNA non-covalently via electrostatic interaction. The higher Kb value of L-tryptophan complex 1 suggested greater DNA binding propensity. Further, to evaluate the mode of action at the molecular level, interaction studies of complexes 1 and 2 with nucleotides (5'-GMP and 5'-TMP) were carried out by UV-vis titrations, 1H and 31P NMR which implicates the preferential selectivity of these complexes to N3 of thymine rather than N7 of guanine. Furthermore, complex 1 exhibits efficient DNA cleavage with supercoiled pBR322. The complex 1 cleaves DNA efficiently involving hydrolytic cleavage pathway. Such chiral synthetic hydrolytic nucleases with asymmetric centers are gaining considerable attention owing to their importance in biotechnology and drug design, in particular to cleave DNA with sequence selectivity different from that of the natural enzymes.

  15. Peripheral Neuropathy and Agent Orange

    Science.gov (United States)

    ... Enter ZIP code here Peripheral Neuropathy and Agent Orange VA presumes Veterans' early-onset peripheral neuropathy is related to their exposure to Agent Orange or other herbicides during service when the disease ...

  16. Agents Play Mix-game

    CERN Document Server

    Gou, C

    2005-01-01

    In mix-game which is an extension of minority game, there are two groups of agents; group1 plays the majority game, but the group2 plays the minority game. This paper studies the change of the average winnings of agents and volatilities vs. the change of mixture of agents in mix-game model. It finds that the correlations between the average winnings of agents and the mean of local volatilities are different with different combinations of agent memory length when the proportion of agents in group 1 increases. This study result suggests that memory length of agents in group1 be smaller than that of agent in group2 when mix-game model is used to simulate the financial markets.

  17. The Power Trading Agent Competition

    OpenAIRE

    Ketter, W.; Collins, J.; REDDY, P; Flath, C.

    2011-01-01

    This is the specification for the Power Trading Agent Competition for 2011 (Power TAC 2011). Agents are simulations of electrical power brokers, who must compete with each other for both power production and consumption, and manage their portfolios.

  18. Amino acids

    Science.gov (United States)

    Amino acids are organic compounds that combine to form proteins . Amino acids and proteins are the building blocks of life. When proteins are digested or broken down, amino acids are left. The human body uses amino acids ...

  19. Chemical cleaning agents and bonding to glass-fiber posts

    Directory of Open Access Journals (Sweden)

    Ana Paula Rodrigues Gonçalves

    2013-02-01

    Full Text Available The influence of chemical cleaning agents on the bond strength between resin cement and glass-fiber posts was investigated. The treatments included 10% hydrofluoric acid, 35% phosphoric acid, 50% hydrogen peroxide, acetone, dichloromethane, ethanol, isopropanol, and tetrahydrofuran. Flat glass-fiber epoxy substrates were exposed to the cleaners for 60 s. Resin cement cylinders were formed on the surfaces and tested in shear. All treatments provided increased bond strength compared to untreated control specimens. All failures were interfacial. Although all agents improved the bond strength, dichloromethane and isopropanol were particularly effective.

  20. Mediating Performance Through Virtual Agents

    OpenAIRE

    Giannachi, Gabriella; Gillies, Marco; Kaye, Nick; Swapp, David

    2009-01-01

    This paper presents the process of creation of virtual agents used in a virtual reality performance. The performance aimed to investigate how drama and performance could inform the creation of virtual agents and also how virtual reality could raise questions for drama and performance. The virtual agents were based on the performance of 2 actors. This paper describes the process of preparing the actors, capturing their performances and transferring them to the virtual agents. A second set of a...

  1. Erythropoietic Agents and the Elderly

    OpenAIRE

    Agarwal, Neeraj; Prchal, Josef T.

    2008-01-01

    Erythropoietin is a peptide hormone that stimulates erythropoiesis. There are several agents in clinical use and in development, which either act as ligands for the cell surface receptors of erythropoietin or promote erythropoietin production that stimulates erythropoiesis. These are known as erythropoietic agents. The agents already in use include epoetin alfa, epoetin beta, and darbepoetin alfa. Newer agents stimulating erythropoiesis (such as continuous erythropoietin receptor activator (C...

  2. Cultural Differentiation of Negotiating Agents

    NARCIS (Netherlands)

    Hofstede, G.J.; Jonker, C.M.; Verwaart, D.

    2012-01-01

    Negotiations proceed differently across cultures. For realistic modeling of agents in multicultural negotiations, the agents must display culturally differentiated behavior. This paper presents an agent-based simulation model that tackles these challenges, based on Hofstede’s model of national cultu

  3. Cultural differentiation of negotiating agents

    NARCIS (Netherlands)

    Hofstede, G.J.; Jonker, C.M.; Verwaart, T.

    2010-01-01

    Negotiations proceed differently across cultures. For realistic modeling of agents in multicultural negotiations, the agents must display culturally differentiated behavior. This paper presents an agent-based simulation model that tackles these challenges, based on Hofstede’s model of national cultu

  4. Collaborating with Autonomous Agents

    Science.gov (United States)

    Trujillo, Anna C.; Cross, Charles D.; Fan, Henry; Hempley, Lucas E.; Motter, Mark A.; Neilan, James H.; Qualls, Garry D.; Rothhaar, Paul M.; Tran, Loc D.; Allen, B. Danette

    2015-01-01

    With the anticipated increase of small unmanned aircraft systems (sUAS) entering into the National Airspace System, it is highly likely that vehicle operators will be teaming with fleets of small autonomous vehicles. The small vehicles may consist of sUAS, which are 55 pounds or less that typically will y at altitudes 400 feet and below, and small ground vehicles typically operating in buildings or defined small campuses. Typically, the vehicle operators are not concerned with manual control of the vehicle; instead they are concerned with the overall mission. In order for this vision of high-level mission operators working with fleets of vehicles to come to fruition, many human factors related challenges must be investigated and solved. First, the interface between the human operator and the autonomous agent must be at a level that the operator needs and the agents can understand. This paper details the natural language human factors e orts that NASA Langley's Autonomy Incubator is focusing on. In particular these e orts focus on allowing the operator to interact with the system using speech and gestures rather than a mouse and keyboard. With this ability of the system to understand both speech and gestures, operators not familiar with the vehicle dynamics will be able to easily plan, initiate, and change missions using a language familiar to them rather than having to learn and converse in the vehicle's language. This will foster better teaming between the operator and the autonomous agent which will help lower workload, increase situation awareness, and improve performance of the system as a whole.

  5. Anti-scaling agents in kraft pulping

    Directory of Open Access Journals (Sweden)

    Felissia, F. E.

    2007-05-01

    Full Text Available Scale formation in the digester during kraft pulping represents a great problem in pulp mills. Scaling reduces pulping control and efficiency, increasing energy costs and leading to cleaning breakdowns, with subsequent losses in productivity. The kraft process promotes CaCO3 scaling due to high calcium ion and carbonate concentrations, as well as high alkalinity and temperature levels, which increase the speed with which liquors reach a state of supersaturation. This work examines the action of diethylene triamine penta(methylene phosphonic acid (DTPMPA, either alone or combined with commercial anti-scaling agents, as an inhibitor of calcium carbonate precipitation in the kraft pulping of Pinus taeda. The theoretical amount of calcium deposited in the digester was obtained by mass balance. Soluble calcium was stable throughout cooking when using the phosphonates alone or combined with anti-scaling agents. When adding only DTPMPA, calcium stays in the pulp, rather than forming deposits.

  6. Agentes de información Information Agents

    Directory of Open Access Journals (Sweden)

    Alfonso López Yepes

    2005-12-01

    Full Text Available Este artículo realiza un repaso sobre las tipologías de agentes de información y describe aspectos como movilidad, racionalidad y adaptatividad, y el ajuste final de estos conceptos a entornos distribuidos como Internet, donde este tipo de agentes tienen un amplio grado de aplicación. Asimismo, se propone una arquitectura de agentes para un sistema multiagente de recuperación de información donde se aplica un paradigma documental basado en el concepto de ciclo documental.This article summarizes the main information agent types reflecting on issues such as mobility, rationality, adaptability and the final adjustment of this concepts to distributed environments such as the Internet, where this kind of agents has wide range application. Likewise, an information agent architecture is proposed to create a multi-agent information retrieval system in which a documentary paradigm based on the documentary cycle is developed.

  7. Secure Mobile Trade Agent

    Directory of Open Access Journals (Sweden)

    Musbah M. Aqe

    2007-01-01

    Full Text Available E-commerce on the internet has the ability to produce millions of transactions and a great number of merchants whose supply merchandise over the internet. As a result, it is difficult for entities to roam over every site on the internet and choose the best merchandise to trade. So, in this paper we introduced a mobile trade agent that visit the sites to gather and evaluate the information from merchant servers and decide to trade goods on behalf of the user. We observed that the combination of public key cryptosystem with distributed object technology make this proposed scheme more secure and efficient than the already existed schemes.

  8. Configuring Computational Agents

    Czech Academy of Sciences Publication Activity Database

    Beuster, G.; Neruda, Roman

    Halifax : Saint Mary's University, 2004 - (Zhuge, H.; Cheung, W.; Liu, J.), s. 57-62 ISBN 0-9734039-8-5. [International Workshop on Knowledge Grid and Grid Intelligence /2./. Beijing (CN), 20.09.2004] R&D Projects: GA AV ČR 1ET100300419 Grant ostatní: CZ-DE project(XX) CZE-03/023 Institutional research plan: CEZ:AV0Z1030915 Keywords : Bang 3 * multi-agent systems * computational intelligence models Subject RIV: BA - General Mathematics

  9. Nitrous acid damage to duplex deoxyribonucleic acid: distinction between deamination of cytosine residues and a novel mutational lesion.

    OpenAIRE

    Frankel, A D; Duncan, B K; Hartman, P E

    1980-01-01

    The rate of nitrous acid deamination of labeled cytosine residues in native Escherichia coli deoxyribonucleic acid was monitored in vitro by release of acid-soluble counts after treatment with uracil deoxyribonucleic acid glycosylase. The reaction exhibited a lag and was not stimulate by several agents previously shown to enhance base substitution mutagenesis during nitrous acid treatment of duplex deoxyribonucleic acid. We conclude that a significant proportion of nitrous acid induced mutage...

  10. Holograms as Teaching Agents

    Science.gov (United States)

    Walker, Robin A.

    2013-02-01

    Hungarian physicist Dennis Gabor won the Pulitzer Prize for his 1947 introduction of basic holographic principles, but it was not until the invention of the laser in 1960 that research scientists, physicians, technologists and the general public began to seriously consider the interdisciplinary potentiality of holography. Questions around whether and when Three-Dimensional (3-D) images and systems would impact American entertainment and the arts would be answered before educators, instructional designers and students would discover how much Three-Dimensional Hologram Technology (3DHT) would affect teaching practices and learning environments. In the following International Symposium on Display Holograms (ISDH) poster presentation, the author features a traditional board game as well as a reflection hologram to illustrate conventional and evolving Three-Dimensional representations and technology for education. Using elements from the American children's toy Operation® (Hasbro, 2005) as well as a reflection hologram of a human brain (Ko, 1998), this poster design highlights the pedagogical effects of 3-D images, games and systems on learning science. As teaching agents, holograms can be considered substitutes for real objects, (human beings, organs, and animated characters) as well as agents (pedagogical, avatars, reflective) in various learning environments using many systems (direct, emergent, augmented reality) and electronic tools (cellphones, computers, tablets, television). In order to understand the particular importance of utilizing holography in school, clinical and public settings, the author identifies advantages and benefits of using 3-D images and technology as instructional tools.

  11. Amphoteric surface active agents

    Directory of Open Access Journals (Sweden)

    Eissa, A.M. F.

    1995-10-01

    Full Text Available 2-[trimethyl ammonium, triethyl ammonium, pyridinium and 2-amino pyridinium] alkanoates, four series of surface active agents containing carbon chain C12, C14, C16 and C18carbon atoms, were prepared. Their structures were characterized by microanalysis, infrared (IR and nuclear magnetic resonance (NMR. Surface and interfacial tension, Krafft point, wetting time, emulsification power, foaming height and critical micelle concentration (cmc were determined and a comparative study was made between their chemical structure and surface active properties. Antimicrobial activity of these surfactants was also determined.

    Se prepararon cuatro series de agentes tensioactivos del tipo 2-[trimetil amonio, trietil amonio, piridinio y 2-amino piridinio] alcanoatos, que contienen cadenas carbonadas con C12, C14, C16 y C18 átomos de carbono.
    Se determinaron la tensión superficial e interfacial, el punto de Krafft, el tiempo humectante, el poder de emulsionamiento, la altura espumante y la concentración critica de miscela (cmc y se hizo un estudio comparativo entre la estructura química y sus propiedades tensioactivas. Se determinó también la actividad antimicrobiana de estos tensioactivos. Estas estructuras se caracterizaron por microanálisis, infrarrojo (IR y resonancia magnética nuclear (RMN.

  12. Contrast agents for MRI

    International Nuclear Information System (INIS)

    Contrast agents are divided into two categories. The first one is paramagnetic compounds, including lanthanides like gadolinium, which mainly reduce the longitudinal (T1) relaxation property and result in a brighter signal. The second class consists of super-paramagnetic magnetic nanoparticles (SPMNPs) such as iron oxides, which have a strong effect on the transversal (T2) relaxation properties. SPMNPs have the potential to be utilized as excellent probes for magnetic resonance imaging (MRI). For instance, clinically benign iron oxide and engineered ferrite nanoparticles provide a good MRI probing capability for clinical applications. Furthermore, the limited magnetic property and inability to escape from the reticuloendothelial system (RES) of the used nanoparticles impede their further advancement. Therefore, it is necessary to develop the engineered magnetic nanoparticle probes for the next-generation molecular MRI. Considering the importance of MRI in diagnosing diseases, this paper presents an overview of recent scientific achievements in the development of new synthetic SPMNP probes whereby the sensitive and target-specific observation of biological events at the molecular and cellular levels is feasible. - Highlights: • This paper studies the contrast agents for MRI. • Fe―Co alloys and Mn-ferrites exhibit suitable contrast enhancement. • Nonhydrolytic thermal-decomposition synthetic method is suitable to produce MNPs. • This method allows controlling the size, magnetic dopants, magneto-crystalline anisotropy. • The increase in the superparamagnetic size leads to the contrast-enhancement

  13. Agent-oriented Software Engineering

    Institute of Scientific and Technical Information of China (English)

    GUAN Xu; CHENG Ming; LIU Bao

    2001-01-01

    An increasing number of computer systems are being viewed in terms of autonomous agents.Most people believe that agent-oriented approach is well suited to design and build complex systems. Yet. todate, little effort had been devoted to discuss the advantages of agent-oriented approach as a mainstreamsoftware engineering paradigm. Here both of this issues and the relation between object-oriented and agent-oriented will be argued. we describe an agent-oriented methodology and provide a quote for designing anauction system.

  14. Comparison of Carboxylic and Hydroxycarboxylic Acids as Complexing Agents for Transition Metal Separation with Nonaqueous Capillary Electrophoresis%非水毛细管电泳分离过渡金属羧酸和羟基羧酸配位剂的比较

    Institute of Scientific and Technical Information of China (English)

    屈锋; 林金明

    2004-01-01

    @@ Many papers have been published on the analysis of metal cations by capillary electrophoresis (CE), for example, lanthanide, transition metal, alkali, and alkaline earth metal ions. Separations of metal ions are based on the differences in their electrophoretic mobilities. Since most metal ions having identical charge and size give rise to identical electrophoretic mobilities, the direct electrophoretic separation of these ions is impossible. However, their mobilities can be modified by introducing chemical equilibria in which the ions are involved in forming complexes. If metal ions have different complex formation constants, their apparent electrophoretic mobilities differ. The separation process is mainly carried out by using various weak complexing agents[1-4], which complex the metal ions to different extents. The weak complexing agents for metal ion separation primarily are hydroxycarboxylic acids with hydroxyl and carboxyl groups. In addition, organic solvents have also been added into the electrolytes to improve the selectivity of metal ion separation. When a metal ion interacts with polar solvent molecules through ion-dipole bonds, a solvation shell may be formed around the central ion. In principle, the solvent solvates all kinds of ions in solution, some to a greater extent than others, depending on the specific properties of the central ion regarding a certain solvent. The use of pure nonaqueous systems offers potential for adjustment of relative migration rates via changes in solvent-ion interaction. Evidence for such analyte-electrolyte interaction has been reported for the separations of inorganic anions[5] and alkali, alkaline earth and transition metal ions in pure nonaqueous systems[6-8].

  15. Learning models of intelligent agents

    Energy Technology Data Exchange (ETDEWEB)

    Carmel, D.; Markovitch, S. [Computer Science Dept., Haifa (Israel)

    1996-12-31

    Agents that operate in a multi-agent system need an efficient strategy to handle their encounters with other agents involved. Searching for an optimal interactive strategy is a hard problem because it depends mostly on the behavior of the others. In this work, interaction among agents is represented as a repeated two-player game, where the agents` objective is to look for a strategy that maximizes their expected sum of rewards in the game. We assume that agents` strategies can be modeled as finite automata. A model-based approach is presented as a possible method for learning an effective interactive strategy. First, we describe how an agent should find an optimal strategy against a given model. Second, we present an unsupervised algorithm that infers a model of the opponent`s automaton from its input/output behavior. A set of experiments that show the potential merit of the algorithm is reported as well.

  16. Flexible, secure agent development framework

    Science.gov (United States)

    Goldsmith; Steven Y.

    2009-04-07

    While an agent generator is generating an intelligent agent, it can also evaluate the data processing platform on which it is executing, in order to assess a risk factor associated with operation of the agent generator on the data processing platform. The agent generator can retrieve from a location external to the data processing platform an open site that is configurable by the user, and load the open site into an agent substrate, thereby creating a development agent with code development capabilities. While an intelligent agent is executing a functional program on a data processing platform, it can also evaluate the data processing platform to assess a risk factor associated with performing the data processing function on the data processing platform.

  17. Scope of Hydrolysable Tannins as Possible Antimicrobial Agent.

    Science.gov (United States)

    Ekambaram, Sanmuga Priya; Perumal, Senthamil Selvan; Balakrishnan, Ajay

    2016-07-01

    Hydrolysable tannins (HTs) are secondary metabolites from plants, which are roughly classified into gallotannins and ellagitannins having gallic acid and ellagic acid residues respectively attached to the hydroxyl group of glucose by ester linkage. The presence of hexahydroxydiphenoyl and nonahydroxyterphenoyl moieties is considered to render antimicrobial property to HTs. HTs also show considerable synergy with antibiotics. Nevertheless, they have low pharmacokinetic property. The present review presents the scope of HTs as future antimicrobial agent. Copyright © 2016 John Wiley & Sons, Ltd. PMID:27062587

  18. Ethylenediaminetetraacetic acid in endodontics.

    Science.gov (United States)

    Mohammadi, Zahed; Shalavi, Sousan; Jafarzadeh, Hamid

    2013-09-01

    Ethylenediaminetetraacetic acid (EDTA) is a chelating agent can bind to metals via four carboxylate and two amine groups. It is a polyamino carboxylic acid and a colorless, water-soluble solid, which is widely used to dissolve lime scale. It is produced as several salts, notably disodium EDTA and calcium disodium EDTA. EDTA reacts with the calcium ions in dentine and forms soluble calcium chelates. A review of the literature and a discussion of the different indications and considerations for its usage are presented. PMID:24966721

  19. Extraction of Heavy Metals from Sludge Using Biodegradable Chelating Agent N,N-bis(carboxymethyl) Glutamic Acid Tetrasodium%生物可降解螯合剂谷氨酸 N,N -二乙酸四钠对污泥中重金属萃取效率的研究

    Institute of Scientific and Technical Information of China (English)

    吴青; 崔延瑞; 汤晓晓; 杨慧娟; 孙剑辉

    2015-01-01

    N, N-bis ( carboxymethyl) glutamic acid tetrasodium ( GLDA), a novel biodegradable and green chelating agent, has excellent metal chelating ability. Batch experiment was conducted to study the extraction process of Cd, Ni, Cu and Zn in industrial sludge using GLDA. The effects of contact time, pH of the system, content of chelating agent were investigated, and the forms of heavy metals in sludge pre- and post-extraction using the modified BCR sequential extraction procedure were studied. The results showed that GLDA was effective for cadmium extraction in sludge. Several heavy metals could be effectively extracted under the condition of pH 4 and molar ratio of chelating agent to total heavy metal 3: 1. Residual fraction took the largest fraction in Zn, which caused the low extraction efficiency of this metal. Chelating properties were related not only to contact time, pH, chelating agent’s concentration, and stability constant but also to species distribution of metals.%谷氨酸 N,N -二乙酸四钠(GLDA)具有较强金属螯合能力,是新一代生物可降解绿色螯合剂。通过分批提取实验对GLDA 去除工业污泥中 Cd、 Ni、 Cu、 Zn 的萃取过程进行研究,考察了萃取时间、萃取体系 pH 值、螯合剂用量等因素对重金属萃取效果的影响,并采用修正的 BCR 连续提取法分析萃取前后污泥中重金属的形态。结果表明, GLDA 对污泥中 Cd 具有良好的去除效果;体系在 pH =4,螯合剂与重金属总量摩尔比为3:1的条件下,多种重金属取得最佳萃取效果; Zn 主要以残渣态存在,导致该金属萃取率低;螯合能力不仅与萃取时间,萃取体系 pH 值,螯合剂用量,螯合常数等因素有关,而且还与金属的形态分布有关。

  20. New concept in nutrition for the maintenance of the aging eye redox regulation and therapeutic treatment of cataract disease; synergism of natural antioxidant imidazole-containing amino acid-based compounds, chaperone, and glutathione boosting agents: a systemic perspective on aging and longevity emerged from studies in humans.

    Science.gov (United States)

    Babizhayev, Mark A

    2010-01-01

    Cataract, opacification of the lens, is one of the commonest causes of loss of useful vision during aging, with an estimated 16 million people world-wide affected. The role of nutritional supplementation in prevention of onset or progression of ocular disease is of interest to health care professionals and patients. The aging eye seems to be at considerable risk from oxidative stress. This review outlines the potential role of the new nutritional strategy on redox balance in age-related eye diseases and detail how the synergism and interaction of imidazole-containing amino acid-based compounds (nonhydrolized L-carnosine, histidine), chaperone agents (such as, L-carnosine, D-pantethine), glutathione-boosting agents (N-acetylcysteine, vitamin E, methionine), and N-acetylcarnosine eye drops plays key roles in the function and maintenance of the redox systems in the aging eye and in the treatment of human cataract disease. A novel patented oral health supplement is presented which enhances the anticataract activity of eye drops and activates functional visual acuity. The clinical data demonstrate the effectiveness and safety of a combined oral health care treatment with amino acids possessing chaperone-like activity with N-acetylcarnosine lubricant eye drops. L-carnosine and N-acetylcarnosine protected the chaperone activity of alpha-crystallin and reduced the increased posttranslational modifications of lens proteins. Biological activities of the nonhydrolyzed carnosine in the oral formulation are based on its antioxidant and antiglycating (transglycating) action that, in addition to heavy metal chelation and pH-buffering ability, makes carnosine an essential factor for preventing sight-threatening eye disorders having oxidative stress in their pathogenesis, neurodegeneration, and accumulation of senile features. The findings suggest that synergism is required between carnosine or other imidazole-containing compounds and reduced glutathione in tissues and cells for