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Sample records for acetylsalicylic acid

  1. Spherical agglomeration of acetylsalicylic acid

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    Polowczyk Izabela

    2016-01-01

    Full Text Available In this paper spherical agglomeration of acetylsalicylic acid was described. In the first step, the system of good and poor solvents as well as bridging liquid was selected. As a result of a preliminary study, ethyl alcohol, water and carbon tetrachloride were used as the good solvent, poor one, and bridging liquid, respectively. Then, the amount of acetylsalicylic acid and the ratio of the solvents as well as the volume of the bridging liquid were examined. In the last step, the agglomeration conditions, such as mixing intensity and time, were investigated. The spherical agglomerates obtained under optimum conditions could be subjected to a tableting process afterwards.

  2. [Interaction between NSAIDs and acetylsalicylic acid disregarded].

    Science.gov (United States)

    Vollaard, E J; Kramers, C; Brouwers, J R B J

    2014-01-01

    In 2013 the European Medicines Agency declared that diclofenac is contraindicated in patients with arterial thrombotic complications, based on a meta-analysis of randomised controlled trials on the adverse reactions of NSAIDs. The same decision was taken for coxibs some years earlier. The Dutch authorities (CBG/MEB) informed physicians and pharmacists about this decision without taking into account whether these patients were using prophylactic acetylsalicylic acid or not. It has been shown that NSAIDs with high COX-1 affinity like ibuprofen and naproxen cause a pharmacodynamic interaction with the inhibition of thromboxane synthesis by acetylsalicylic acid. This interaction does not occur with relatively COX-2-selective NSAIDs such as coxibs and diclofenac. Therefore, in patients who use acetylsalicylic acid for thromboprophylaxis, contraindicating coxibs or diclofenac is not justified, on the contrary: they are preferable.

  3. [The forensic chemical investigation of acetylsalicylic acid].

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    Shormanov, V K; Chupak, V V; Pobedonstseva, M N; Maslov, S V; Kibets, N A; Tikhopoeva, N N

    2015-01-01

    The objective of the present study was to develop the universal approach to the quantitative determination of acetylsalicylic acid in biological tissues and fluids to be applied in the practice of forensic chemical expertise with the use of thin-layer chromatography, gas chromatography and mass spectrometry, low-pressure column chromatography, and spectrophotometry. A system of solvents consisting of acetone and ethyl acetate (7:3) was proposed as a universal agent for extracting acetylsalicylic acid from the cadaveric tissues and blood. It was shown that acetylsalicylic acid and its principal metabolite, salicylic acid, can be purified from the endogenous admixtures present in the biological materials by column chromatography on silica gel L 40/100 mcm. Salicylic acid in extracts from biological materials was identified and quantified with the use of thin-layer chromatography, gas chromatography/mass spectrometry, and electronic spectrophotometry. The method for forensic chemical investigation of acetylsalicylic acid has been developed and applied in the analysis of the material provided for expertise.

  4. ACETYLSALICYLIC ACID IN RHEUMATOLOGY: NEW EVIDENCE

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    Yuri Vladimirovich Muravyev

    2013-01-01

    Full Text Available Acetylsalicylic acid that has long widely used in rheumatoid arthritis and condemned by rheumatologists to oblivion since the late 20th century and it may take its rightful place in the treatment of both rheumatoid arthritis and other rheumatic diseases.

  5. Synthesis and transdermal properties of acetylsalicylic acid and selected esters

    OpenAIRE

    2006-01-01

    The primary aim of this study was to determine the transdermal penetration of acetylsalicylic acid and some of its derivatives, to establish a correlation, if any, with selected physicochemical properties and to determine if transdermal application of acetylsalicylic acid and its derivatives will give therapeutic drug concentrations with respect to transdermal flux. Ten derivatives of acetylsalicylic acid were prepared by esterification of acetylsalicyloyl chloride with ten different alcohols...

  6. Determination of acetylsalicylic acid and salicylic acid in foods, using HPLC with fluorescence detection.

    OpenAIRE

    Venema, D.P.; Hollman, P.C.H.; Janssen, P.L.T.M.K.; Katan, M B

    1996-01-01

    We developed a specific and sensitive HPLC method with fluorescence detection for the determination of free acetylsalicylic acid, free salicylic acid, and free salicylic acid plus salicylic acid after alkaline hydrolysis (free-plus-bound) in foods. Acetylsalicylic acid was detected after postcolumn hydrolysis to salicylic acid. With the method for free acetylsalicylic acid and salicylic acid, recovery was 95-98␏or acetylsalicylic acid added to foods and 92-102␏or salicylic acid. Recovery of a...

  7. Synthesis and transdermal properties of acetylsalicylic acid and selected esters.

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    Gerber, Minja; Breytenbach, Jaco C; Hadgraft, Jonathan; du Plessis, Jeanetta

    2006-03-01

    The primary aim of this study was to determine the transdermal penetration of acetylsalicylic acid and some of its derivatives, to establish a correlation, if any, with selected physicochemical properties and to determine if transdermal application of acetylsalicylic acid and its derivatives will give therapeutic drug concentrations with respect to transdermal flux. Ten derivatives of acetylsalicylic acid were prepared by esterification of acetylsalicyloyl chloride with ten different alcohols. The experimental aqueous solubility, logD and transdermal flux values were determined for acetylsalicylic acid and its derivatives at pH 4.5. In vitro penetration was measured through excised female human abdominal skin in diffusion cells. The experimental aqueous solubility of acetylsalicylic acid (6.56 mg/ml) was higher than that of the synthesised acetylsalicylate derivatives (ranging from 1.76 x 10(-3) to 3.32 mg/ml), and the logD of acetylsalicylic acid (-0.85) was lower than that of its derivatives (ranging from -0.25 to 1.95). There was thus an inverse correlation between the aqueous solubility data and the logD values. The experimental transdermal flux of acetylsalicylic acid (263.83 nmol/cm(2)h) was much higher than that of its derivatives (ranging from 0.12 to 136.02 nmol/cm(2)h).

  8. Polymorphisms in genes encoding acetylsalicylic acid metabolizing enzymes are unrelated to upper gastrointestinal health in cardiovascular patients on acetylsalicylic acid.

    NARCIS (Netherlands)

    Oijen, M.G.H. van; Huybers, S.; Peters, W.H.M.; Drenth, J.P.H.; Laheij, R.J.F.; Verheugt, F.W.A.; Jansen, J.B.M.J.

    2005-01-01

    BACKGROUND: As acetylsalicylic acid is metabolized by UDP-glucuronosyltransferase 1A6 (UGT1A6) and cytochrome P450 2C9 (CYP2C9), interindividual differences in activity of these enzymes may modulate the effects and side-effects of acetylsalicylic acid. The objective of this study was to assess wheth

  9. Acetylsalicylic acid: Incoming 150 years of the first synthesis

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    Mijin Dušan Ž.

    2002-01-01

    Full Text Available Acetylsalicylic acid is one of the most fascinating and versatile drugs known to medicine, as well as one of the oldest. Acetylsalicylic acid is a drug which is safe, with analgetic, antirheumatic, anti-inflammatory antiplatelet and antithrombotic action. It may be applied not only in clinical practice, but also as prevention. The first known use of an acetylsalicylic acid-like preparation can be traced to ancient Greece. In 1853 Charles Gerhardt published the first synthesis of acetylsalicylic acid. Felix Hoffmann, a chemist for Friedrich Bayer, a German dye company obtained a patent on acetylsalicylic acid some 40 years later. Bayer coined the name Aspirin for the new product. The 20 in century was the century in which many researchers in many companies tried to improve the synthesis of acetylsalicylic acid not only in terms of yield but also purity. This paper describes the history, use, mechanism of action, synthesis and production as well as the purification and stability of acetylsalicylic acid.

  10. The evaluation method for antiplatelet effect of acetylsalicylic acid.

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    Yokoyama, Haruko; Mastumura, Takashi; Soeda, Shinji; Suzuki, Yuji; Watanabe, Masayuki; Kashiwakura, Emiko; Saso, Takayuki; Ikeda, Noriyuki; Tokuoka, Kentaro; Kitagawa, Yasuhisa; Yamada, Yasuhiko

    2014-12-01

    Reduced platelet aggregation by acetylsalicylic acid administration has been associated with adverse outcomes in patients with thrombotic diseases, thus it is important to determine aspirin resistance in those cases. The antiplatelet effect of acetylsalicylic acid is rarely measured, but it has many problems. The aim of this study was to find the evaluation method for antiplatelet effect after administration of acetylsalicylic acid. We developed a particle counting method based upon laser light scattering, and utilized the platelet aggregation agonists, collagen, at 0.25, 0.5 and 1.0 μg/mL, and adenosine diphosphate (ADP), at 0.5, 1.0 and 2.0 μM, to determine their effective concentrations. Seventeen healthy volunteers were administered acetylsalicylic acid at 162 mg/day, with platelet aggregation determined before and 20 min after administration. In all subjects, the rate of platelet aggregation induced by 1.0 μg/mL of collagen before taking acetylsalicylic acid was the highest value obtained, while 20 min after acetylsalicylic acid administration, aggregation induced by collagen at 1.0 μg/mL was significantly decreased as compared to before administration. As for the other concentrations of collagen and all those of ADP tested, platelet aggregation was either not significantly induced before taking acetylsalicylic acid or the rate of aggregation was not significantly decreased after taking acetylsalicylic acid. Our results indicate that collagen at 1.0 μg/mL is appropriate as a platelet aggregation agonist for evaluating the antiplatelet effect of acetylsalicylic acid. Thus, it is useful that the measurement is performed only once.

  11. Inhibitory effects of acetylsalicylic acid on exocrine pancreatic carcinogenesis.

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    Yıldız, H; Oztas, H; Yıldız, D; Koc, A; Kalipci, E

    2013-05-01

    We investigated short (6 months) and long (12 months) term inhibitory effects of low (200 ppm) and high (400 ppm) dosages of acetylsalicylic acid (aspirin) on exocrine pancreatic carcinogenesis. It is known that exocrine pancreatic carcinogenesis can be detected by the presence of atypical acinar cell foci (AACF) in pancreas. We investigated possible inhibitory effects of acetylsalicylic acid in an azaserine-treated rat model. AACF were produced in rats by injection with azaserine according to previous studies. Our findings showed that the number, volume and diameter of pancreatic AACF were reduced after acetylsalicylic acid application. These observations suggest that acetylsalicylic acid may exert a protective effect against neoplastic development of pancreatic acinar cells in azaserine injected rats. Our findings corroborate reports in the literature concerning the effects of aspirin in reducing neoplastic development.

  12. Acetylsalicylic acid and acetaminophen protect against oxidative neurotoxicity.

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    Maharaj, H; Maharaj, D S; Daya, S

    2006-09-01

    Due to the implication of oxidative stress in neurodegenerative disorders we decided to investigate the antioxidant properties of acetylsalicylic acid and acetaminophen either alone or in combination. The thiobarbituric acid assay (TBA) and the nitroblue tetrazolium (NBT) assay were used to investigate quinolinic acid (QA)-induced: lipid peroxidation and superoxide anion generation in the rat hippocampus, in vivo. The study also shows, using cresyl violet staining, the preservation of structural integrity of neuronal cells following treatment with acetylsalicylic acid and acetaminophen in QA-lesioned rat hippocampus. Furthermore the study sought to determine whether these agents have any effect on endogenous (QA) formation. This study shows that acetylsalicylic acid and acetaminophen inhibit QA-induced superoxide anion generation, lipid peroxidation and cell damage, in vivo, in the rat hippocampus. In addition these agents inhibit the enzyme, 3-hydroxyanthranilic acid oxygenase (3-HAO), responsible for the synthesis of endogenous QA.

  13. Determination of acetylsalicylic acid and salicylic acid in foods, using HPLC with fluorescence detection.

    NARCIS (Netherlands)

    Venema, D.P.; Hollman, P.C.H.; Janssen, P.L.T.M.K.; Katan, M.B.

    1996-01-01

    We developed a specific and sensitive HPLC method with fluorescence detection for the determination of free acetylsalicylic acid, free salicylic acid, and free salicylic acid plus salicylic acid after alkaline hydrolysis (free-plus-bound) in foods. Acetylsalicylic acid was detected after postcolumn

  14. Effect of acetylsalicylic acid on fatty acid omega-hydroxylation in rat liver.

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    Okita, R

    1986-12-01

    The effect of acetylsalicylic acid on the cytochrome P-450-mediated fatty acid omega-hydroxylation system was assessed in male Sprague-Dawley rats after they were fed a diet containing 1% (w/w) acetylsalicylic acid. A 3-fold increase in the specific activity of laurate omega-hydroxylation was observed in the acetylsalicylic acid fed rats in comparison to control rats. This effect of acetylsalicylic acid was unique as the specific activities of other cytochrome P-450-mediated reactions were not increased. The induction of the laurate omega-hydroxylation system was also manifested in a rapid formation of its dicarboxylic acid derivative, dodecanedioic acid, as the omega-hydroxy derivative was further oxidized by alcohol and aldehyde dehydrogenases. These results suggest the acetylsalicylic acid is similar to other peroxisomal proliferating agents in that it also induces the microsomal fatty acid omega-hydroxylation system and may account for the appearance of unique dicarboxylic acids in Reye's syndrome patients.

  15. ACETYLSALICYLIC ACID IN THE PREVENTION OF ATHEROTHROMBOTIC EVENTS

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    A. V. Govorin

    2015-12-01

    Full Text Available The results of large-scale clinical trials have convincingly demonstrated the effectiveness of acetylsalicylic acid (ASA in primary and secondary prevention of atherothrombotic events. Studies on the safety of different ASA formulations have been continuing. Magnesium hydroxide included in combined medicine, Сardiomagnil, prevents ASA adverse effects on the gastric mucosa and reduces in severity of dyspeptic symptoms.

  16. ACETYLSALICYLIC ACID IN THE PREVENTION OF ATHEROTHROMBOTIC EVENTS

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    A. V. Govorin

    2012-01-01

    Full Text Available The results of large-scale clinical trials have convincingly demonstrated the effectiveness of acetylsalicylic acid (ASA in primary and secondary prevention of atherothrombotic events. Studies on the safety of different ASA formulations have been continuing. Magnesium hydroxide included in combined medicine, Сardiomagnil, prevents ASA adverse effects on the gastric mucosa and reduces in severity of dyspeptic symptoms.

  17. ON THE 125TH ANNIVERSARY OF ACETYLSALICYLIC ACID

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    I. N. Bokarev

    2011-01-01

    Full Text Available An experience of acetylsalicylic acid (ASA clinical use since its synthesis in 1887 is highlighted. ASA modes of action and its position among the modern antiplatelet agents are considered. The evidence based clinical data on ASA treatment and the problem of antiplatelet therapy resistance are discussed. ASA interaction with other drugs and ASA pleiotropic effects are reviewed 

  18. Acetylsalicylic acid as an adjuvant therapy for schizophrenia

    NARCIS (Netherlands)

    Laan, Wijnand; Selten, Jean-Paul; Kahn, Rene S.; Huisman, Anne-Margriet; Heijnen, Cobi J.; Grobbee, Diederick E.; Burger, Huibert

    2006-01-01

    Background: Findings from both epidemiological and basic research point to the possibility that NSAIDS impede the deterioration in schizophrenia. Methods: To study the efficacy of acetylsalicylic acid we will perform a randomized placebo controlled double- blind add- on trial of 80 inpatients and ou

  19. Influence of vitamin E on the antiplatelet effect of acetylsalicylic acid in human blood.

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    González-Correa, J A; Arrebola, M M; Guerrero, A; Muñoz-Marín, J; Ruiz-Villafranca, D; Sánchez de La Cuesta, F; De La Cruz, J P

    2005-01-01

    We analysed the in vitro interaction between acetylsalicylic acid and vitamin E on the principal antiplatelet sites of action of acetylsalicylic acid, i.e., platelet aggregation, prostanoid production in platelets and leukocytes, and nitric oxide synthesis. Aggregation was measured in whole blood and in platelet-rich plasma (PRP) with ADP, collagen or arachidonic acid as platelet inducers, and we measured the production of thromboxane B2, prostacyclin and nitric oxide. Vitamin E potentiated the antiplatelet effect of acetylsalicylic acid in both whole blood and PRP. In PRP induced with collagen the IC50 for acetylsalicylic acid alone was 339+/-11.26, and that of acetylsalicylic acid+vitamin E was 0.89+/-0.09 (Pacetylsalicylic acid. Vitamin E spared or even increased prostacyclin levels, and acetylsalicylic acid+vitamin E diminished the inhibition of prostacyclin synthesis by acetylsalicylic acid (IC50 acetylsalicylic acid alone=1.81+/-0.15 microM; IC50 acetylsalicylic acid+vitamin E= 12.92+/-1.10 microM, Pacetylsalicylic acid on neutrophil nitric oxide production 42-fold (Pacetylsalicylic acid in vitro, and thus merits further research in ex vivo studies.

  20. Effects of microgravity on the binding of acetylsalicylic acid by Rhizobium leguminosarum bv. trifolii

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    Urban, James E.; Gerren, Richard; Zoelle, Jeffery

    1995-07-01

    Bacteroids can be induced in vitro by treating growing Rhizobium leguminosarum bv. trifolii with succinic acid or succinic acid structural analogs like acetylsalicylic acid. Quantitating bacteroid induction by measuring acetylsalicylic binding under normal (1 g) conditions showed two forms of binding to occur. In one form of binding cells immediately bound comparatively high levels of acetylsalicylic acid, but the binding was quickly reversed. The second form of binding increased with time by first-order kinetics, and reached saturation in 40 s. Similar experiments performed in the microgravity environment aboard the NASA 930 aircraft showed only one form of binding and total acetylsalicylic acid bound was 32% higher than at 1 g.

  1. Superiority of zinc complex of acetylsalicylic acid to acetylsalicylic acid in preventing postischemic myocardial dysfunction.

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    Korkmaz, Sevil; Atmanli, Ayhan; Li, Shiliang; Radovits, Tamás; Hegedűs, Peter; Barnucz, Enikő; Hirschberg, Kristóf; Loganathan, Sivakkanan; Yoshikawa, Yutaka; Yasui, Hiroyuki; Karck, Matthias; Szabó, Gábor

    2015-09-01

    The pathophysiology of ischemic myocardial injury involves cellular events, reactive oxygen species, and an inflammatory reaction cascade. The zinc complex of acetylsalicylic acid (Zn(ASA)2) has been found to possess higher anti-inflammatory and lower ulcerogenic activities than acetylsalicylic acid (ASA). Herein, we studied the effects of both ASA and Zn(ASA)2 against acute myocardial ischemia. Rats were pretreated with ASA (75 mg/kg) or Zn(ASA)2 (100 mg/kg) orally for five consecutive days. Isoproterenol (85 mg/kg, subcutaneously [s.c.]) was applied to produce myocardial infarction. After 17-22 h, animals were anesthetized with sodium pentobarbital (60 mg/kg, intraperitoneally [i.p.]) and both electrical and mechanical parameters of cardiac function were evaluated in vivo. Myocardial histological and gene expression analyses were performed. In isoproterenol-treated rats, Zn(ASA)2 treatment normalized significantly impaired left-ventricular contractility index (Emax 2.6 ± 0.7 mmHg/µL vs. 4.6 ± 0.5 mmHg/µL, P < 0.05), increased stroke volume (30 ± 3 µL vs. 50 ± 6 µL, P < 0.05), decreased systemic vascular resistance (7.2 ± 0.7 mmHg/min/mL vs. 4.2 ± 0.5 mmHg/min/mL, P < 0.05) and reduced inflammatory infiltrate into the myocardial tissues. ECG revealed a restoration of elevated ST-segment (0.21 ± 0.03 mV vs. 0.09 ± 0.02 mV, P < 0.05) and prolonged QT-interval (79.2 ± 3.2 ms vs. 69.5 ± 2.5 ms, P < 0.05) by Zn(ASA)2. ASA treatment did not result in an improvement of these parameters. Additionally, Zn(ASA)2 significantly increased the mRNA-expression of superoxide dismutase 1 (+73 ± 15%), glutathione peroxidase 4 (+44 ± 12%), and transforming growth factor (TGF)-β1 (+102 ± 22%). In conclusion, our data demonstrate that oral administration of zinc and ASA in the form of bis(aspirinato)zinc(II) complex is superior to ASA in preventing electrical

  2. [Clarification on publications concerning the synthesis of acetylsalicylic acid].

    Science.gov (United States)

    Lafont, O

    1996-01-01

    Charles Frédéric Gerhardt (1816-1856) mentioned in his Traité de chimie Organique (1854) a publication, in French (realized in 1852 but published in 1853) entitled "Researches on anhydrous organic acids" in which, was reported the reaction of sodium salicylate with acetyl chloride. He thought that the reaction product was an acid anhydride, but obtained really crude acetylsalicylic acid. Later on, but also in 1853, a publication in german, by the same author related the same experiments. Surprisingly only the second publication has been mentioned in most of the historical studies on the subject. Acetyl salicylic acid was identified and synthesised in 1859 by von Gilm by another method and the product obtained by Gerhardt was identified to it in 1869.

  3. Acidosis, magnesium and acetylsalicylic acid: Effects on thrombin

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    Borisevich, Nikolaj; Loznikova, Svetlana; Sukhodola, Aleksandr; Halets, Inessa; Bryszewska, Maria; Shcharbin, Dzmitry

    2013-03-01

    Thrombin, an enzyme from the hydrolase family, is the main component of the blood coagulation system. In ischemic stroke it acts as a serine protease that converts soluble fibrinogen into insoluble strands of fibrin forming blood clots in the brain. It has been found to phosphoresce at room temperature in the millisecond and microsecond ranges. The phosphorescence of thrombin was studied under physiological conditions, in acidosis (decrease of pH from 8.0 to 5.0) and on the addition of salts (magnesium sulfate and sodium chloride) and of acetylsalicylic acid, and its connection with thrombin function is discussed. Acidosis significantly increased the internal dynamics of thrombin. We propose that lactate-acidosis plays a protective role in stroke, preventing the formation of clots. The addition of NaCl and MgSO4 in different concentrations increased the internal dynamics of thrombin. Also, the addition of MgSO4 decreased thrombin-induced platelet aggregation. However, magnesium sulfate and acetylsalicylic acid in the therapeutic concentrations used for treatment of ischemic stroke had no effect on thrombin internal dynamics. The data obtained will help to elucidate the conformational stability of thrombin under conditions modulating lactate-acidosis and in the presence of magnesium sulfate.

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

    Science.gov (United States)

    Wójcik, Marek J.

    1981-11-01

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

  5. Flow-injection chemiluminescence determination of acetylsalicylic acid based on its enhancing effect on the lucigenin–hydrogen peroxide system.

    Science.gov (United States)

    Wabaidur, S M; Alam, S M; Alothmana, Z A; Eldesokya, Gaber

    2014-09-01

    A sensitive flow-injection chemiluminescence method for the determination of acetylsalicylic acid is described. It is based on the enhanced chemiluminescent emission of the alkaline lucigenin–H2O2 system by acetylsalicylic acid. The difference in chemiluminescent intensity of alkaline lucigenin–H2O2 in the presence of acetylsalicylic acid from that in the absence of acetylsalicylic acid was linear at acetylsalicylic acid concentrations in the range of 0.0029–47.37 μg/mL, with detection and quantification limits of 0.0011 and 0.0029 μg/mL, respectively. The correlation coefficient of the working curve was 0.9983. The relative standard deviation (n = 10) for 25 μg/mL acetylsalicylic acid is 1.95%. All experimental parameters were optimized. The method was successfully applied to the determination of acetylsalicylic acid in pharmaceutical preparations. The recovery results obtained by the method were satisfactory.

  6. Treatment of endometriosis with local acetylsalicylic acid injection: experimental study in rabbits.

    Science.gov (United States)

    Siqueira, Juliana Menezes; Barreto, Adriana Beatriz; Saad-Hossne, Rogério

    2011-01-01

    The objective of the present study was to estimate the effects of introduction of acetylsalicylic acid solution into peritoneal implants in autologous endometrium as a method for treating endometriosis. Forty adult female rabbits were subdivided into 4 groups of 10 rabbits each, and endometriosis was induced via autotransplantation of endometrial fragments into the peritoneal cavity. At 30 days after induction of endometriosis, all animals were randomly assigned to 1 of 2 protocols. In protocol 1, animals were evaluated at 24 hours after treatment; group 1 (control) received physiologic solution, and group 2 received acetylsalicylic acid. In protocol 2, animals were evaluated at 10 days after treatment, group 3 (control) and group 4 received acetylsalicylic acid. After measuring the lesion, the endometriotic focus was removed and prepared for mounting on slides for histologic analysis. Imaging software was used for analysis of the total remaining area of endometrial tissue. The affected area in acetylsalicylic acid-treated animals was smaller than that in control animals at 24 hours and 10 days after treatment; a significant difference was found between control and treated groups (p acetylsalicylic acid groups (p = .30), and no differences between times (p = .75). Acetylsalicylic acid solution led to less growth (or higher involution) of endometrial implants. Acetylsalicylic acid injected directly into endometriotic foci was effective in their destruction. This presents new perspectives for treatment of endometriosis and for clinical applications based on further clinical studies.

  7. Vanadocene reactions with hydroxy acids. [Hydroxy acids: acetylsalicylic, gallic, lactic, salicyclic, orotic,. gamma. -hydroxybutyric acids

    Energy Technology Data Exchange (ETDEWEB)

    Latyaeva, V.N.; Lineva, A.N.; Zimina, S.V.; Ehllert, O.G.; Arsen' eva, T.I. (Gor' kovskij Meditsinskij Inst. (USSR))

    1984-03-01

    To prepare a series of vanadium cyclopentadienylcarboxylates soluble in water, the vanadocene reactions with lactic, ..gamma..-oxybutyric-, salicylic,- gallic-, orotic-, and acetylsalicylic acids have been studied. To determine the influence of cyclopentadienyl groups, bound with a vanadium atom, on the physiological activity of the complexes formed, vanadium halides are made to react with lactic acid. Only the vanadocene reaction with orotic acid was conducted in an aqueous medium, other interactions were realized in the diethyl ether, toluene, T, H, P medium. The interaction of vanadocene and vanadium halides with lactic-, salicylic-, acetylsalicylic- and gallic acids was found to lead to the formation of water-soluble vanadium complexes of Cp/sub 2/, VOCOR or CpV (OCOR)/sub 2/ type. The data on the produced compounds yield, their IR spectra, decomposition temperatures, solubility, effective magnetic moments are presented.

  8. Acetylsalicylic Acid Daily vs Acetylsalicylic Acid Every 3 Days in Healthy Volunteers: Effect on Platelet Aggregation, Gastric Mucosa, and Prostaglandin E2 Synthesis.

    Science.gov (United States)

    Ferreira, Plinio Minghin Freitas; Gagliano-Jucá, Thiago; Zaminelli, Tiago; Sampaio, Marinalva Ferreira; Blackler, Rory Willian; Trevisan, Miriam da Silva; Novaes Magalhães, Antônio Frederico; De Nucci, Gilberto

    2016-07-01

    Substantial platelet inhibition was observed 3 days after a single administration of acetylsalicylic acid 81 mg to healthy volunteers. Here we investigate prostaglandin E2 (PGE2 ) antrum concentrations and gastrointestinal symptoms in two treatment groups: one receiving losartan and acetylsalicylic acid every day and the other receiving losartan every day and acetylsalicylic acid every 3 days. Twenty-eight healthy volunteers from both sexes received either 50 mg losartan and acetylsalicylic acid 81 mg daily or 50 mg losartan and acetylsalicylic acid 81 every 3 days with placebo on the other days. Therapy was delivered for 30 days for both groups. Gastric endoscopy was performed before and after treatment period. Biopsies were collected for PGE2 quantification. Platelet function tests were carried out before and during treatment and TXB2 release on platelet rich plasma was measured. The every 3 day low-dose acetylsalicylic acid regimen produced complete inhibition of platelet aggregation compared to the daily treatment. Thromboxane B2 release was substantially abolished for both groups during treatment. There was no significant difference on the endoscopic score of both treatment groups after the 30-day treatment (P = .215). There was over 50% suppression of antrum PGE2 content on volunteers receiving acetylsalicylic acid daily (P = .0016), while for the every 3 day dose regimen there was no significant difference between pre and post-treatment antrum PGE2 dosages (P = .4193). Since PGE2 is involved in gastric healing, we understand that this new approach could be safer and as efficient as the standard daily therapy on a long-term basis.

  9. High-pressure polymorphism of acetylsalicylic acid (aspirin): Raman spectroscopy

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    Crowell, Ethan L.; Dreger, Zbigniew A.; Gupta, Yogendra M.

    2015-02-01

    Micro-Raman spectroscopy was used to elucidate the high-pressure polymorphic behavior of acetylsalicylic acid (ASA), an important pharmaceutical compound known as aspirin. Using a diamond anvil cell (DAC), single crystals of the two polymorphic phases of aspirin existing at ambient conditions (ASA-I and ASA-II) were compressed to 10 GPa. We found that ASA-I does not transform to ASA-II, but instead transforms to a new phase (ASA-III) above ∼2 GPa. It is demonstrated that this transformation primarily introduces structural changes in the bonding and arrangement of the acetyl groups and is reversible upon the release of pressure. In contrast, a less dense ASA-II shows no transition in the pressure range studied, though it appears to exhibit a disordered structure above 7 GPa. Our results suggest that ASA-III is the most stable polymorph of aspirin at high pressures.

  10. [Comparative assessment of antiaggregant efficacy of acetylsalicylic acid and clopidogrel in peripheral atherosclerosis].

    Science.gov (United States)

    Kuznetsov, M R; Sergeeva, N A; Koshkin, V M; Boldin, B V; Rodionov, S V; Virganskiĭ, A O; Kosykh, I V; Lisenkov, O P; Kuznetsova, V F

    2014-01-01

    Presented in the article are the results of studying antiaggregate activity of acetylsalicylic acid and clopidogrel in a total of 36 patients suffering from various-severity chronic arterial insufficiency of lower limbs on the background of atherosclerosis obliterans. The study was conducted prior to treatment for correct selection of a particular antiplatelet agent. The obtained results showed that clopidogrel was not always more efficient than acetylsalicylic acid, since there is individual sensitivity of each patients to a particular antiplatelet agent. Therefore, an individual approach is necessary to conservative therapy of arterial insufficiency of lower limbs. For some patients it is preferable to administer clopidogrel, for others - acetylsalicylic acid. In a series of cases combined treatment is justified, while some patients having low sensitivity to both acetylsalicylic acid and clopidogrel require careful selection of alternative agents influencing other thrombocyte receptors.

  11. [Identification of rat and human hemoglobin acetilation sites after its interaction with acetylsalicylic acid].

    Science.gov (United States)

    Shreĭner, E V; Murashko, E A; Dubrovskiĭ, Ia D; Krasnov, N V; Podol'skaia, E P; Babakov, V N

    2012-01-01

    The possibility of interaction of 0.1 mg/mL acetylsalicylic acid with purified human and rat globin in vitro during 24 h at 37 degrees C was investigated. The rat globin can be modified with acetylsalicylic acid on aminoacid residues K-17, K-57, K-91, K-140 in alpha subunit as well as on K-18, K-77 in beta subunit. The human globin can be modified with acetylsalicylic acid on aminoacid residues K-17, K-41, K-57 and K-91 in alpha subunit as well as on K-18, K-96 and K- 133 in beta subunit. We identified of acetetylated lysines K-17 and K-57 in alpha subunit of human hemoglobin after incubation whole blood with 0.1 mg/mL acetylsalicylic acid during 3 h.

  12. Maternal use of acetaminophen, ibuprofen, and acetylsalicylic acid during pregnancy and risk of cryptorchidism

    DEFF Research Database (Denmark)

    Jensen, Morten Søndergaard; Rebordosa, Cristina; Thulstrup, Ane Marie

    2010-01-01

    Cyclooxygenase (COX) inhibitors-acetaminophen, ibuprofen and acetylsalicylic acid-have endocrine-disruptive properties in the rainbow trout. In humans, aspirin blocks the androgen response to human chorionic gonadotropin (hCG), and, because hCG-stimulated androgen production in utero is crucial...... for normal testicular descent, exposure to COX inhibitors at vulnerable times during gestation may impair testicular descent. We examined whether prenatal exposure to acetaminophen, ibuprofen, and acetylsalicylic acid was associated with increased occurrence of cryptorchidism....

  13. Acetylsalicylic acid induces programmed cell death in Arabidopsis cell cultures.

    Science.gov (United States)

    García-Heredia, José M; Hervás, Manuel; De la Rosa, Miguel A; Navarro, José A

    2008-06-01

    Acetylsalicylic acid (ASA), a derivative from the plant hormone salicylic acid (SA), is a commonly used drug that has a dual role in animal organisms as an anti-inflammatory and anticancer agent. It acts as an inhibitor of cyclooxygenases (COXs), which catalyze prostaglandins production. It is known that ASA serves as an apoptotic agent on cancer cells through the inhibition of the COX-2 enzyme. Here, we provide evidences that ASA also behaves as an agent inducing programmed cell death (PCD) in cell cultures of the model plant Arabidopsis thaliana, in a similar way than the well-established PCD-inducing agent H(2)O(2), although the induction of PCD by ASA requires much lower inducer concentrations. Moreover, ASA is herein shown to be a more efficient PCD-inducing agent than salicylic acid. ASA treatment of Arabidopsis cells induces typical PCD-linked morphological and biochemical changes, namely cell shrinkage, nuclear DNA degradation, loss of mitochondrial membrane potential, cytochrome c release from mitochondria and induction of caspase-like activity. However, the ASA effect can be partially reverted by jasmonic acid. Taking together, these results reveal the existence of common features in ASA-induced animal apoptosis and plant PCD, and also suggest that there are similarities between the pathways of synthesis and function of prostanoid-like lipid mediators in animal and plant organisms.

  14. Acetylsalicylic acid protects erectile function in diabetic rats.

    Science.gov (United States)

    Hafez, G; Gonulalan, U; Kosan, M; Arioglu, E; Ozturk, B; Cetinkaya, M; Gur, S

    2014-01-01

    We aimed to evaluate the effect of acetylsalicylic acid (ASA) treatment on diabetes-induced erectile dysfunction. Adult male Sprague-Dawley rats were divided into four groups as follows: (i) control (C), (ii) diabetic (D), (iii) ASA-treated control (C+ASA) and (iv) ASA-treated diabetic (D+ASA) groups. In groups 2 and 4, diabetes was induced by injection of 35 mg kg(-1) streptozotocin. ASA (100 mg kg(-1) day(-1) , orally) was administrated to rats in groups 3 and 4 for 8 weeks. Both intracavernosal pressure (ICP) and mean arterial blood pressure (MAP) were measured in in vivo studies. In organ bath, the relaxation responses to acetylcholine (ACh), electrical field stimulation (EFS) and sodium nitroprusside were tested in corpus cavernosum (CC) strips. The mRNA expression for neuronal nitric oxide synthase (nNOS) was calculated using reverse transcription polymerase chain reaction technique. In in vivo experiments, diabetic rats displayed reduced ICP/MAP values, which were normalised with ASA treatment. The relaxant response to high-dose ACh and EFS at low frequencies (1-8 Hz) in CC strips from the D+ASA group were significantly higher when compared to the D group. Treatment with ASA normalised the raised mRNA expressions of nNOS in diabetic penile tissues. ASA may be involved in mRNA of protein synthesis of NO released from nonadrenergic and noncholinergic cavernosal nerve in diabetes.

  15. Acetylsalicylic acid as a potential pediatric health hazard: legislative aspects concerning accidental intoxications in the European Union.

    Science.gov (United States)

    Mund, Menen E; Gyo, Christoph; Brüggmann, Dörthe; Quarcoo, David; Groneberg, David A

    2016-01-01

    Acetylsalicylic acid is a frequently used medication worldwide. It is not used in pediatrics due its association with Reye syndrome. However, in case of pediatric intoxication, children are more fragile to salicylate poisoning because of their reduced ability of buffer the acid stress. Intoxication leads to a decoupling of oxidative phosphorylation and subsequently to a loss in mitochondrial function. Symptoms of poisoning are diverse; eventually they can lead to the death of the patient. Governmental websites of various EU countries were searched for legal information on acetylsalicylic acid availability in pharmacies and non-pharmacy stores. Various EU countries permit prescription-free sales of acetylsalicylic acid in pharmacies and non-pharmacy stores. In Sweden acetylsalicylic acid 500 mg may be sold in a maximum package size of 20 tablets or effervescent tablets in a non-pharmacy. In the UK a maximum of 16 tablets of acetylsalicylic acid 325 mg is allowed to sell in non-pharmacies. In Ireland acetylsalicylic acid is classified as S2 medication. Subsequently, acetylsalicylic acid is allowed to be sold prescription-free in pharmacies and non-pharmacy stores. In the Netherlands acetylsalicylic acid may only be sold in drug stores or pharmacies. A maximum of 24 tablets of 500 mg is allowed to purchase in a drug store. Several countries in the European Union are permitted to offer acetylsalicylic acid prescription-free in pharmacies and non-pharmacy stores without legal guidance on the storage position within the store. Further research is needed to investigate whether acetylsalicylic acid is located directly accessible to young children within the stores in EU countries which permit prescription-free sales of acetylsalicylic acid.

  16. Acetylsalicylic acid and labeling of blood constituents with technetium-99m

    Energy Technology Data Exchange (ETDEWEB)

    Fonseca, Adenilson de Souza da [Universidade do Estado, Rio de Janeiro, RJ (Brazil). Dept. de Farmacologia e Psicobiologia; Frydman, Jacques Natan Grinapel; Rocha, Vanessa Camara da; Bernardo-Filho, Mario [Universidade do Estado, Rio de Janeiro, RJ (Brazil). Inst. de Biologia Roberto Alcantara Gomes. Dept. de Biofisica e Biometria

    2005-10-15

    Acetylsalicylic acid is the drug most used an anti-inflammatory agent and for secondary prevention of thrombotic phenomenon. Drugs can modify the labeling of blood constituents with technetium-99m (99m Tc). The aim of this work was to evaluate the effect of in vitro or in vivo assays with acetylsalicylic acid on the labeling of the blood constituents with 99m Tc. In vitro assay was performed with samples of whole blood from Wistar rats incubated with acetylsalicylic acid (1.0 mg/ml) for one hour before the 99m Tc-labeling process. For in vivo assay, Wistar rats were treated with acetylsalicylic acid (1.5 mg/kg) during one hour, and the whole blood was withdrawn for the 99m Tc-labeling process. Saline was used in control groups. Data showed that the fixation of 99m Tc to the blood constituents was not significantly (p>0.05) modified in in vitro and in vivo assays with acetylsalicylic acid, at least not when the experiments were carried out with the doses normally used in human beings. (author)

  17. Effect of acetylsalicylic acid on microvascular thrombosis in autologous breast reconstruction.

    Science.gov (United States)

    Enajat, Morteza; Aziz Mohammadi, Mujzgan; Debeij, Jan; van der Hulst, Rene R W J; Mureau, Marc A M

    2014-01-01

    Although advances in microsurgery have increased success rates of autologous breast reconstruction, microvascular thrombosis still remains a major concern as a cause of flap failure. At present, no evidence-based guidelines on pharmacological prevention of microvascular thrombosis exist. This study investigates the effect of acetylsalicylic acid on the incidence of microvascular complications in patients undergoing autologous breast reconstruction. Patients undergoing deep inferior epigastric artery perforator or free transverse rectus abdominis myocutaneous flap breast reconstruction at two academic centers in the Netherlands between 2005 and 2011 were included. Patients at one center received once daily 0.6 mL of nadroparine and 40 mg acetylsalicylic acid, while patients at the other center received 0.6 mL nadroparine only. A total of 430 consecutive patients underwent 592 breast reconstructions. No statistically significant differences were found between the two groups in the incidence of flap failure (2.8 and 2.5%), microvascular thromboembolic complications (2.6 and 3.8%), venous congestion (3.4 and 2.8%), or overall complications (28.0 and 32.3%). Hematoma tended to occur more often in the group receiving acetylsalicylic acid (9.2 and 4.7%).It was found that no protective effect of acetylsalicylic acid on microvascular complications was present. Given its known risks and the somewhat increased occurrence of hematoma in the present study, we stopped to routinely administer acetylsalicylic acid after autologous breast reconstruction.

  18. Synergistic inhibitory effect of ascorbic acid and acetylsalicylic acid on prostaglandin E2 release in primary rat microglia.

    Science.gov (United States)

    Fiebich, Bernd L; Lieb, Klaus; Kammerer, Norbert; Hüll, Michael

    2003-07-01

    Ascorbic acid (vitamin C) has been suggested to protect cerebral tissue in a variety of pathophysiological situations such as head trauma, ischemia or Alzheimer's disease. Most of these protective actions have been attributed to the antioxidative capacity of ascorbic acid. Besides the presence of elevated levels of oxygen radicals, prostaglandins produced by neurones and microglial cells seem to play an important role in prolonged tissue damage. We investigated whether ascorbic acid alone inhibits prostaglandin E2 (PGE2) synthesis and may augment the inhibitory effect of acetylsalicylic acid on prostaglandin synthesis. Ascorbic acid dose-dependently inhibited PGE2 synthesis in lipopolysaccharide-treated primary rat microglial cells (IC50 = 3.70 micro m). In combination with acetylsalicylic acid (IC50 = 1.85 micro m), ascorbic acid augmented the inhibitory effect of acetylsalicylic acid on PGE2 synthesis (IC50 = 0.25 micro m in combination with 100 micro m ascorbic acid). Ascorbic acid alone or in combination with acetylsalicylic acid did not inhibit cyclooxygenase-2 (COX-2) protein synthesis but inhibited COX-2 enzyme activity. Our results show that ascorbic acid and acetylsalicylic acid act synergistically in inhibiting PGE2 synthesis, which may help to explain a possible protective effect of ascorbic acid in various brain diseases.

  19. Acetylsalicylic Acid and Eflornithine in Treating Patients at High Risk for Colorectal Cancer | Division of Cancer Prevention

    Science.gov (United States)

    This phase II trial is studying how well giving acetylsalicylic acid together with eflornithine works in treating patients at high risk for colorectal cancer. Chemoprevention is the use of certain drugs to keep cancer from forming. The use of acetylsalicylic acid and eflornithine may prevent colorectal cancer. |

  20. Modified MCM-41 as a drug delivery system for acetylsalicylic acid

    Science.gov (United States)

    Vyskočilová, Eliška; Luštická, Ivana; Paterová, Iva; Machová, Libuše; Červený, Libor

    2014-12-01

    The modification of prepared MCM-41 by different groups (amino, chloro and oxo) was studied. Prepared materials were treated by acetylsalicylic acid and hybrid materials were characterized, compared from the point of view of immobilized amount of active substance. The highest amount of acetylsalicylic acid was detected using methyl-tert- butyl ether as a solvent and MCM-41 without modification after 1 h (0.35 g per 1 g of the support) or MCM modified by amino group after 5 h (0.37 g per 1 g of the support) as a support. Using amino modified MCM, the longer treatment by acetylsalicylic acid converged to the equilibrium and after 24 h the immobilized amount was 0.3 g per 1 g. A dissolution in vitro study was carried out, comparing the stability of formed interactions. The slowest dissolution was detected using non-modified MCM-41 and oxo modified material.

  1. Relaxation in the glass former acetylsalicylic acid studied by deuteron magnetic resonance and dielectric spectroscopy

    Science.gov (United States)

    Nath, R.; El Goresy, T.; Geil, B.; Zimmermann, H.; Böhmer, R.

    2006-08-01

    Supercooled liquid and glassy acetylsalicylic acid was studied using dielectric spectroscopy and deuteron relaxometry in a wide temperature range. The supercooled liquid is characterized by major deviations from thermally activated behavior. In the glass the secondary relaxation exhibits the typical features of a Johari-Goldstein process. Via measurements of spin-lattice relaxation times the selectively deuterated methyl group was used as a sensitive probe of its local environments. There is a large difference in the mean activation energy in the glass with respect to that in crystalline acetylsalicylic acid. This can be understood by taking into account the broad energy barrier distribution in the glass.

  2. Heat shock protein 70-dependent protective effect of polaprezinc on acetylsalicylic acid-induced apoptosis of rat intestinal epithelial cells.

    Science.gov (United States)

    Qin, Ying; Naito, Yuji; Handa, Osamu; Hayashi, Natsuko; Kuki, Aiko; Mizushima, Katsura; Omatsu, Tatsushi; Tanimura, Yuko; Morita, Mayuko; Adachi, Satoko; Fukui, Akifumi; Hirata, Ikuhiro; Kishimoto, Etsuko; Nishikawa, Taichiro; Uchiyama, Kazuhiko; Ishikawa, Takeshi; Takagi, Tomohisa; Yagi, Nobuaki; Kokura, Satoshi; Yoshikawa, Toshikazu

    2011-11-01

    Protection of the small intestine from mucosal injury induced by nonsteroidal anti-inflammatory drugs including acetylsalicylic acid is a critical issue in the field of gastroenterology. Polaprezinc an anti-ulcer drug, consisting of zinc and L-carnosine, provides gastric mucosal protection against various irritants. In this study, we investigated the protective effect of polaprezinc on acetylsalicylic acid-induced apoptosis of the RIE1 rat intestinal epithelial cell line. Confluent rat intestinal epithelial cells were incubated with 70 µM polaprezinc for 24 h, and then stimulated with or without 15 mM acetylsalicylic acid for a further 15 h. Subsequent cellular viability was quantified by fluorometric assay based on cell lysis and staining. Acetylsalicylic acid-induced cell death was also qualified by fluorescent microscopy of Hoechst33342 and propidium iodide. Heat shock proteins 70 protein expression after adding polaprezinc or acetylsalicylic acid was assessed by western blotting. To investigate the role of Heat shock protein 70, Heat shock protein 70-specific small interfering RNA was applied. Cell viability was quantified by fluorometric assay based on cell lysis and staining and apoptosis was analyzed by fluorescence-activated cell sorting. We found that acetylsalicylic acid significantly induced apoptosis of rat intestinal epithelial cells in a dose- and time-dependent manner. Polaprezinc significantly suppressed acetylsalicylic acid-induced apoptosis of rat intestinal epithelial cells at its late phase. At the same time, polaprezinc increased Heat shock protein 70 expressions of rat intestinal epithelial cells in a time-dependent manner. However, in Heat shock protein 70-silenced rat intestinal epithelial cells, polaprezinc could not suppress acetylsalicylic acid -induced apoptosis at its late phase. We conclude that polaprezinc-increased Heat shock protein 70 expression might be an important mechanism by which polaprezinc suppresses acetylsalicylic

  3. EFFECTS OF ASCORBIC ACID AND ACETYLSALICYLIC ACID SUPPLEMENTATION ON THE PERFORMANCE OF BROILER CHICKS EXPOSED TO HEAT STRESS

    Directory of Open Access Journals (Sweden)

    B. Anwar, S. A. Khan, A. Aslam, A. Maqbool1 and K. A. Khan

    2004-07-01

    Full Text Available A total of 100, day-old broiler chicks were randomly divided into 5 equal groups and kept under elevated temperature (93-97oF to see the effect of ascorbic acid and acetylsalicylic acid on the feed conversion ratio (FCR, immune status and ratio of weight of bursa, thymus and spleen to body weight. Heat stress increased the FCR but decreased the immune response and ratio of bursa, thymus and spleen to body weight of the birds. Ascorbic acid and acetylsalicylic acid supplementation during heat stress had beneficial effects on FCR, immune status and ratio of bursa, thymus and spleen to body weight. Grossly, bursa, thymus and spleen of heat stressed birds were atrophied but in ascorbic acid and acetylsalicylic acid supplemented birds these organs were not atrophied. No specific histopathological changes were observed in all groups.

  4. Enteric coating can lead to reduced antiplatelet effect of low-dose acetylsalicylic acid

    DEFF Research Database (Denmark)

    Fentz Haastrup, Peter; Grønlykke, Thor; Jarbøl, Dorte Ejg

    2015-01-01

    Low-dose acetylsalicylic acid (ASA) is widely used as antithrombotic prophylaxis. Enteric coated ASA has been developed in order to decrease the risk of gastrointestinal side effects. The consequences of enteric coating on pharmacokinetics and antiplatelet effect of ASA have not systematically been...

  5. Risk of haemorrhage from transurethral prostatectomy in acetylsalicylic acid and NSAID-treated patients

    DEFF Research Database (Denmark)

    Wierød, F S; Frandsen, N J; Jacobsen, J D

    1998-01-01

    Postoperative bleeding in patients who regularly ingest acetylsalicylic acid (ASA) has been reported after several types of surgery. However, data on the influence of ASA on the risk of haemorrhage from transurethral prostatectomy (TUR-P) have been conflicting. We have studied retrospectively...

  6. ACETYLSALICYLIC ACID IN LOW DOSES FOR SECONDARY PREVENTION OF CARDIO-VASCULAR COMPLICATIONS

    Directory of Open Access Journals (Sweden)

    N. A. Dmitrieva

    2009-01-01

    Full Text Available Data of evidence based medicine which confirm efficacy of acetylsalicylic acid (ACA in cardiologic practice are presented. The special attention is given to generic drugs of ACA. Their application has increased essentially recently. Some of generics are comparable with original drugs on clinical efficacy but have economic advantages.

  7. Determination of acetylsalicylic acid and its major metabolites in bovine urine using ultra performance liquid chromatography.

    Science.gov (United States)

    Castillo-García, M L; Aguilar-Caballos, M P; Gómez-Hens, A

    2015-03-15

    A new method based on ultra high performance liquid chromatography (UPLC) with photometric and fluorometric detection for the determination of acetylsalicylic acid and its main metabolites, namely gentisic, salicylic and salicyluric acids, in bovine urine samples is reported. Photometric detection was used for acetylsalicylic acid determination, whereas the native fluorescence of the metabolites was monitored using fluorometric detection. The separation was performed under isocratic conditions, using acetonitrile-phosphate solution (3.5mM, pH 3.5) (26:74, v/v) as the mobile phase. The retention times of the four compounds were lower than 2min, which are shorter than those achieved using conventional HPLC. Under the optimum separation conditions, the dynamic ranges and detection limits (ngmL(-1)) were: 0.2-2500, 0.09 for gentisic acid; 0.2-2500, 0.08 for salicylic acid and 2.5-15,000, 1.1 for salicyluric acid, using fluorescence detection, and 10-25,000, 2.2 for acetylsalicylic acid, using UV detection. Intra-day and inter-day precision data were assessed at two levels of concentration of each analyte using both detection systems. The selectivity of the method was checked by assaying different drugs of veterinary use showing that most of them did not interfere with the determination of the analytes. The method has been applied to the analysis of bovine urine samples, which only required a simple clean up step of the samples prior to injection in the UPLC system. A recovery study was performed, which provided values in the range of 80-100%. This fact proves the practical usefulness of this method as an ultrafast analytical tool for the therapeutic control of acetylsalicylic acid administration in bovine animals intended for food production.

  8. Prolongation of bleeding time and inhibition of platelet aggregation by low-dose acetylsalicylic acid in patients with cerebrovascular disease

    DEFF Research Database (Denmark)

    Boysen, G; Boss, A H; Ødum, Niels

    1984-01-01

    Platelet aggregation and bleeding time was measured in 43 cerebrovascular patients participating in a controlled double-blind study of low-dose acetylsalicylic acid. In 19 patients with satisfactory inhibition of the platelet aggregation obtained by 50 to 70 mg acetylsalicylic acid per day...... the bleeding time averaged 11.2 minutes in contrast to 7.0 minutes in the placebo group, p less than 0.001. This study confirms our previous findings of platelet inhibition by low-dose acetylsalicylic acid in patients with cerebrovascular disease. The prolongation of the bleeding time demonstrates that we...... are dealing not merely with an in vitro phenomenon but with a significant in vivo effect. The study provides the rationale for clinical evaluations of low-dose acetylsalicylic acid in stroke prophylaxis....

  9. Stimulation of cysteinyl leukotriene production in mast cells by heat shock and acetylsalicylic acid.

    Science.gov (United States)

    Mortaz, Esmaeil; Redegeld, Frank A; Dunsmore, Kathy; Odoms, Kelli; Wong, Hector R; Nijkamp, Frans P; Engels, Ferdi

    2007-04-30

    Immunoglobulin (Ig) E-dependent activation of mast cells is central to the allergic response. The engagement of IgE-occupied receptors initiates a series of molecular events that causes the release of preformed, and de novo synthesis of, allergic mediators. Cysteinyl leukotrienes are able to contract airway smooth muscle and increase mucus secretion and vascular permeability and recruit eosinophils. Mast cells have also recently been recognized as active participants in innate immune responses. Heat stress can modulate innate immunity by inducing stress proteins such as heat-shock proteins (HSPs). We previously demonstrated that treatment of mast cells with heat shock or acetylsalicylic acid results in an increase of TNF-alpha and IL-6 release. This effect was paralleled by expression of HSP70. In the current study, we further investigated the effects of heat shock and acetylsalicylic acid on the activation of mast cells and the release of cysteinyl leukotrienes. In mouse mast cells, derived from a culture of bone marrow cells, responsiveness to heat shock, acetylsalicylic acid and exogenous or endogenous HSP70 was monitored by measuring leukotriene C4 release. We show that after heat shock treatment and exposure to acetylsalicylic acid leukotriene production was increased. Moreover, exogenous rHSP70 also induced leukotriene production. Because it has been reported that leukotriene production in mast cells may be mediated by Toll like receptor (TLR) activation, and HSP70 also activates TLRs signaling, we further explored these issues by using mast cells that are not able to produce HSP70, i.e. heat shock factor-1 (HSF-1) knockout cells. We found that in HSF-1 knockout bone marrow derived mast cells, heat shock and acetylsalicylic acid failed to induce release of leukotrienes. Moreover, in wild type cells the surface expression of TLR4 was attenuated, whereas the intracellular expression was up-regulated. We conclude that heat shock and acetylsalicylic acid induce

  10. Burden of upper gastrointestinal symptoms in patients receiving low-dose acetylsalicylic acid for cardiovascular risk management

    DEFF Research Database (Denmark)

    Bytzer, Peter; Pratt, Stephen; Elkin, Eric

    2013-01-01

    Continuous low-dose acetylsalicylic acid (aspirin; ASA) is a mainstay of cardiovascular (CV) risk management. It is well established, however, that troublesome upper gastrointestinal (GI) symptoms are commonly experienced among low-dose ASA users.......Continuous low-dose acetylsalicylic acid (aspirin; ASA) is a mainstay of cardiovascular (CV) risk management. It is well established, however, that troublesome upper gastrointestinal (GI) symptoms are commonly experienced among low-dose ASA users....

  11. Acetylsalicylic Acid Compared to Placebo in Treating High-Risk Patients With Subsolid Lung Nodules | Division of Cancer Prevention

    Science.gov (United States)

    This randomized phase II trial studies acetylsalicylic acid compared to placebo in treating high-risk patients with subsolid lung nodules. A nodule is a growth or lump that may be malignant (cancer) or benign (not cancer). Chemoprevention is the use of drugs to keep cancer from forming or coming back. The use of acetylsalicylic acid may keep cancer from forming in patients with subsolid lung nodules. |

  12. Preparation of acetylsalicylic acid-acylated chitosan as a novel polymeric drug for drug controlled release.

    Science.gov (United States)

    Liu, Changkun; Wu, Yiguang; Zhao, Liyan; Huang, Xinzheng

    2015-01-01

    The acetylsalicylic acid-acylated chitosan (ASACTS) with high degree of substitution (DS) was successfully synthesized, and characterized with FTIR, (1)H NMR and elemental analysis methods. The optimum synthesis conditions were obtained which gave the highest DS (about 60%) for ASACTS. Its drug release experiments were carried out in simulated gastric and intestine fluids. The results show that the drugs in the form of acetylsalicylic acid (ASA) and salicylic acid (SA) were released in a controlled manner from ASACTS only in simulated gastric fluid. The release profile can be best fitted with logistic and Weibull model. The research results reveal that ASACTS can be a potential polymeric drug for the controlled release of ASA and SA in the targeted gastric environment.

  13. DNA damage and oxidative stress induced by acetylsalicylic acid in Daphnia magna.

    Science.gov (United States)

    Gómez-Oliván, Leobardo Manuel; Galar-Martínez, Marcela; Islas-Flores, Hariz; García-Medina, Sandra; SanJuan-Reyes, Nely

    2014-08-01

    Acetylsalicylic acid is a nonsteroidal anti-inflammatory widely used due to its low cost and high effectiveness. This compound has been found in water bodies worldwide and is toxic to aquatic organisms; nevertheless its capacity to induce oxidative stress in bioindicators like Daphnia magna remains unknown. This study aimed to evaluate toxicity in D. magna induced by acetylsalicylic acid in water, using oxidative stress and DNA damage biomarkers. An acute toxicity test was conducted in order to determine the median lethal concentration (48-h LC50) and the concentrations to be used in the subsequent subacute toxicity test in which the following biomarkers were evaluated: lipid peroxidation, oxidized protein content, activity of the antioxidant enzymes superoxide dismutase, catalase, and glutathione peroxidase, and level of DNA damage. Lipid peroxidation level and oxidized protein content were significantly increased (pacetylsalicylic acid induces oxidative stress and DNA damage in D. magna.

  14. Pharmacological Correction of the Negative Effect of Acetylsalicylic Acid on the Energy-Generating System

    Directory of Open Access Journals (Sweden)

    Vladimir V. Udut, ScD

    2012-03-01

    Full Text Available The present paper demonstrates the effect of ASA and its combination with SUC on the energy-producing system of rat heart mitochondria as well as an assessment of SUC preventive application effect on ASA pharmacokinetic parameters. Experiments conducted on outbred male albino rats (200-250 g on a model of a xenobiotic load induced by seven days of intragastric injections of acetylsalicylic acid at a dose of 250 mg/kg have shown inhibition of the oxygen consumption rates in the heart mitochondria as well as a limitation of the succinate-dependent substrate oxidation pathways and a decrease in the mitochondria ATP/ADP coefficient. Succinic acid (50 mg/kg for 7 days was injected as a preventive medication to correct the mitochondrial bioenergetics revealed. A comparative research of the pharmacokinetics of acetylsalicylic acid and acetylsalicylic acid against the background of succinic acid performed on the model of rabbits has shown total similarity in the parameters analyzed. This fact demonstrates the possibility of prevention of mitochondrial dysfunction using the intermediate Krebs cycle. SUC as preventive medication promotes the elimination of ASA-induced negative metabolic shifts in the rat heart mitochondria by normalizing the succinate- and NAD-dependent respiration, oxidative phosphorylation, and therefore, it finds good use in the correction of ASA-induced negative side-effects of an energy-generating system

  15. Teratogenicity studies with methotrexate, aminopterin, and acetylsalicylic acid in domestic cats.

    Science.gov (United States)

    Khera, K S

    1976-08-01

    Pregnancy was timed in cats following induced ovulation. Methotrexate, (0.5 mg/kg), aminopterin, (0.1 mg/kg), and acetylsalicylic acid, (25 or 50 mg/kg) were administered orally in gelatin capsules in single daily doses on different days of gestation, methotrexate (MTX) on days 11-14, 14-17, or 17-20, aminopterin on day 12, 14, or 16, and acetylsalicylic acid (ASA) on days 10-15 or 15-20. Maternal toxicity was produced only by MTX. MTX given on days 11-14 and 14-17 produced high frequencies of malformations including umbilical hernia. Aminopterin caused no conclusive teratogenic response. An overall increased frequency of anomalies occurred after 50 mg/kg ASA but no single anomaly predominated.

  16. The effects of acetylsalicylic acid on the pituitary prolactin of the lizard, Uromastix hardwickii.

    Science.gov (United States)

    Ahmad, Mahmood; Hasan, Ruqaiya; Ahmad, Mansoor; Qureshi, Anila; Masroor, Shama

    2005-07-01

    This study deals with the intravenous administration of 7 mg acetylsalicylic acid (ASA) solution to Uromastix hardwickii for 4 days. It enhances the activity of anterior pituitary lactotrophs, when 0.1 ml of pituitary homogenate of ASA treated was injected hypodermically to crop-sac showed a greater diametric response and increased activity with milk like secretion than that of the injections of 0.1 ml homogenate of control pituitary. The present study indicated that ASA induces hyperprolactinemia.

  17. Activity ratio between antiprostacyclin and antiaggregating effects of acetylsalicylic acid, indometacin and ditazole.

    Science.gov (United States)

    Caprino, L; Togna, G; Antonetti, F; Borrelli, F

    1980-01-01

    The effects of acetylsalicylic acid (ASA) indometacin and ditazole on prostacyclin production from rabbit aortic rings were studied in comparison to their inhibiting activity on platelet aggregation. The result were expressed as the ratio between the drug dose inhibiting by 50% prostacycline production and the minimum oral antiaggregating dose. The following ratios were found: 2.4 for ASA, 7.3 for indometacin and 20.4 for ditazole.

  18. [Acetylsalicylic acid desensitization in the new era of percutaneous coronary intervention].

    Science.gov (United States)

    Fuertes Ferre, Georgina; Ferrer Gracia, Maria Cruz; Calvo Cebollero, Isabel

    2015-09-21

    Dual antiplatelet therapy is essential in patients undergoing percutaneous coronary intervention with stent implantation. Hypersensitivity to acetylsalicylic acid (ASA) limits treatment options. Desensitization to ASA has classically been studied in patients with respiratory tract disease. Over the last years, many protocols have been described about ASA desensitization in patients with ischemic heart disease, including acute coronary syndrome and the need for coronary stent implantation. It is important to know the efficacy and safety of ASA desensitization in these patients.

  19. Gastro-duodenal ulcers with perforation caused by short-term acetylsalicylic acid ingestion: Case report

    Directory of Open Access Journals (Sweden)

    Ćulafić Đorđe

    2009-01-01

    Full Text Available Introduction. Acetylsalicylic acid ingestion may cause serious gastrointestinal toxicity, in particular bleeding or perforated peptic ulcer. Case Outline. A 72-year-old male patient presented with diffuse abdominal pain, malaise, and dark stools. Several days before hospitalization, he had cerebrovascular insult and began to use acetylsalicylic acid of 100 mg per day. In physical findings a diffusely painful sensitivity of the abdomen was detected on palpation. Laboratory findings revealed hyposideremic anaemia with inflammatory syndrome. Native abdominal x-ray did not show the presence of pneumoperitoneum. Upper endoscopy of the gastric corpus and antrum revealed several ulcerations 10-11 mm in diameter covered with fibrin, with bleeding ulceration in the angulus region of the lesser gastric curvature. The bulbus was oedematous and hyperaemic with a perforated ulcer on the anterior wall. Upper central laparotomy showed a perforated duodenal bulbus. The posterior wall of the bulbus was normal, while the anterior wall was without scarring. Given the general condition of the patient and local findings, interrupted suture of the ulcer was performed with omentoplasty. Postoperative course was uneventful. A peroral diet was initiated on the 4th postoperative day, and the patient was discharged on the 8th postoperative day. Conclusion. Elderly people who use acetylsalicylic acid in prophylaxis should take it in lower doses, with proton pump inhibitors, especially during the first two months.

  20. Determination of acetylsalicylic acid in commercial tablets by SERS using silver nanoparticle-coated filter paper

    Science.gov (United States)

    Sallum, Loriz Francisco; Soares, Frederico Luis Felipe; Ardila, Jorge Armando; Carneiro, Renato Lajarim

    2014-12-01

    In this work, filter paper was used as a low cost substrate for silver nanoparticles in order to perform the detection and quantification of acetylsalicylic acid by SERS in a commercial tablet. The reaction conditions were 150 mM of ammonium hydroxide, 50 mM of silver nitrate, 500 mM of glucose, 12 min of the reaction time, 45 °C temperature, pretreatment with ammonium hydroxide and quantitative filter paper (1-2 μm). The average size of silver nanoparticles deposited on the paper substrate was 180 nm. Adsorption time of acetylsalicylic acid on the surface of the silver-coated filter paper was studied and an adsorption time of 80 min was used to build the analytical curve. It was possible to obtain a calibration curve with good precision with a coefficient of determination of 0.933. The method proposed in this work was capable to quantify acetylsalicylic acid in commercial tablets, at low concentration levels, with relative error of 2.06% compared to the HPLC. The preparation of filter paper coated with silver nanoparticles using Tollen's reagent presents several advantages such as low cost of synthesis, support and reagents; minimum amount of residuals, which are easily treated, despite the SERS spectroscopy presenting fast analysis, with low sample preparation and low amount of reactants as in HPLC analysis.

  1. Acetylsalicylic acid combined with diclofenac inhibits cartilage degradation in rabbit models of osteoarthritis.

    Science.gov (United States)

    Liu, Jianqiang; Wu, Changshun; Wang, Dong; Wang, Laicheng; Sun, Shui

    2016-10-01

    The present study aimed to investigate the effect of different concentrations of acetylsalicylic acid combined with diclofenac on the articular cartilage of a rabbit model of osteoarthritis (OA). A total of 40 New Zealand white rabbits were divided into 5 groups. Group A was a sham-operated control group, which was treated with normal saline. Groups B-E were OA models and were treated with normal saline and acetylsalicylic acid combined with diclofenac at concentrations of 5, 10 and 20 mg/kg, respectively. A cartilage macroscopic examination and a pathological observation were performed to analyze the structure of the articular cartilage in all of the treated groups. The nitric oxide (NO) content and interleukin 1β (IL-1β) levels were detected by an enzyme-linked immunosorbent assay. In addition, the protein expression of matrix metalloproteinase 3 (MMP)-3 and MMP-13 were detected by western blot analysis. The mRNA expression of tissue inhibitor of metalloproteinases 1 (TIMP1) was detected by polymerase chain reaction (PCR). The results revealed that different concentrations of the drugs significantly reduced the scores of cartilago articularis, the NO and IL-1β levels and the protein expression of MMP-3 and MMP-13. Furthermore, PCR revealed that the mRNA expression of TIMP1 was significantly upregulated, and the effects increased with increasing drug concentration. Thus, the administration of different concentrations of acetylsalicylic acid combined with diclofenac demonstrates preventive or therapeutic effects against OA progression.

  2. Successful living donor liver transplantation for acute liver failure after acetylsalicylic acid overdose.

    Science.gov (United States)

    Shirota, Tomoki; Ikegami, Toshihiko; Sugiyama, Satoshi; Kubota, Kouji; Shimizu, Akira; Ohno, Yasunari; Mita, Atsuyoshi; Urata, Koichi; Nakazawa, Yuichi; Kobayashi, Akira; Iwaya, Mai; Miyagawa, Shinichi

    2015-04-01

    A 20-year-old woman was admitted to an emergency hospital after ingesting 66 g of acetylsalicylic acid in a suicide attempt. Although she was treated with gastric lavage, oral activated charcoal, and intravenous hydration with sodium bicarbonate, her hepatic and renal function gradually deteriorated and serum amylase levels increased. Steroid pulse therapy, plasma exchange, and continuous hemodiafiltration did not yield any improvement in her hepatic or renal function, and she was transferred to our hospital for living donor liver transplantation. Nine days after drug ingestion, she developed hepatic encephalopathy: thus, we diagnosed the patient with acute liver failure with hepatic coma accompanied by acute pancreatitis due to the overdose of acetylsalicylic acid. Living donor liver transplantation was immediately performed using a left lobe graft from the patient's mother. Following transplantation, the patient's renal and hepatic function and consciousness improved, and she was discharged. In this report, we describe a rare case of acetylsalicylic acid-induced acute liver failure with acute hepatic coma and concomitant acute pancreatitis and acute renal failure, which were treated successfully with emergency living donor liver transplantation.

  3. An investigation about the solid state thermal degradation of acetylsalicylic acid: polymer formation

    Energy Technology Data Exchange (ETDEWEB)

    Silva, Edna M. de A; Melo, Dulce M. de A; Moura, Maria de F.V. de; Farias, Robson F. de

    2004-05-06

    An investigation about the thermal degradation of acetylsalicylic acid (ASA) is performed. It is verified that the thermal degradation of ASA produces not only salicylic acid (SA) and acetic acid (AA) as products but also an ASA polymer, which is transparent and solid. And also verified that the temperature in which the polymer is obtained influences its physical consistence (solid or semi-solid). Furthermore, the ASA polymer is very stable from a thermic point of view, as verified by TG and DSC analysis. X-ray diffraction patterns obtained for the ASA polymer show that it exhibits a low crystallinity.

  4. EFFECTS OF ACETYLSALICYLIC ACID AND CLOPIDOGREL ON MORPHOFUNCTIONAL STATUS OF ERYTHROCYTES IN PATIENTS WITH ACUTE CORONARY SYNDROME

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    A. L. Alyavi

    2016-01-01

    Full Text Available Aim. In patients with acute coronary syndrome (ACS to study an aggregation activity and morphology of erythrocytes and to assess their changes during therapy with acetylsalicylic acid, clopidogrel and combined antiplatelet therapy (acetylsalicylic acid and clopidogrel.Material and methods. 98 patients (67 men and 31 women, aged 59,6±10,8 y.o. with ACS were included in the study. Patients were split in 3 groups depending on prescribed antiplatelets (acetylsalicylic acid; clopidogrel; acetylsalicylic acid+clopidogrel. Aggregation activity and morphofunctional status of erythrocytes were evaluated at baseline, after 3 and 7 days of treatment.Results. The highest efficacy of antiaggregant therapy was observed in patients receiving antiplatelet combination. In this group there was a maximal reduction of erythrocyte aggregation and a number of pathological erythrocytes in peripheral blood by the 3rd day of therapy. This effect was increasing by the 7th day.Conclusion. The effect of all antiplatelet drugs was significant. The antiaggregant effect of clopidogrel was more significant than this for acetylsalicylic acid. Efficacy of combined therapy was higher than these for each drug alone. 

  5. EFFECTS OF ACETYLSALICYLIC ACID AND CLOPIDOGREL ON MORPHOFUNCTIONAL STATUS OF ERYTHROCYTES IN PATIENTS WITH ACUTE CORONARY SYNDROME

    Directory of Open Access Journals (Sweden)

    A. L. Alyavi

    2009-01-01

    Full Text Available Aim. In patients with acute coronary syndrome (ACS to study an aggregation activity and morphology of erythrocytes and to assess their changes during therapy with acetylsalicylic acid, clopidogrel and combined antiplatelet therapy (acetylsalicylic acid and clopidogrel.Material and methods. 98 patients (67 men and 31 women, aged 59,6±10,8 y.o. with ACS were included in the study. Patients were split in 3 groups depending on prescribed antiplatelets (acetylsalicylic acid; clopidogrel; acetylsalicylic acid+clopidogrel. Aggregation activity and morphofunctional status of erythrocytes were evaluated at baseline, after 3 and 7 days of treatment.Results. The highest efficacy of antiaggregant therapy was observed in patients receiving antiplatelet combination. In this group there was a maximal reduction of erythrocyte aggregation and a number of pathological erythrocytes in peripheral blood by the 3rd day of therapy. This effect was increasing by the 7th day.Conclusion. The effect of all antiplatelet drugs was significant. The antiaggregant effect of clopidogrel was more significant than this for acetylsalicylic acid. Efficacy of combined therapy was higher than these for each drug alone. 

  6. [New biological active derivatives of indomethacin and acetylsalicylic acid. Synthesis, physico-chemical characterisation and structure validation].

    Science.gov (United States)

    Stan, Catalina; Stefanache, Alina; Dumitrache, M

    2006-01-01

    It is well known that niflumic acid glycinamide has a good antiinflammatory action useful in gum inflammatory diseases. The objective of this study was to obtain new glycinamides of acetylsalicylic acid and indomethacin, which could have a better antiinflammatory action than niflumic acid glycinamide. The study presents the synthesis, physico-chemical characterisation and structure validation of these glycinamides.

  7. The combination of acetylsalicylic acid and dipyridamole is more effective in secondary prevention following transient ischaemic attack or cerebral infarction: The debate is closed

    NARCIS (Netherlands)

    Luijckx, G.J.; De Keyser, J.H.A.

    2006-01-01

    The European/Australasian stroke prevention in reversible ischaemia trial (ESPRIT) confirms that long-term administration of the combination acetylsalicylic acid and dipyridamole is more effective than acetylsalicylic acid in reducing the risk of vascular events after cerebral ischaemia of arterial

  8. Use of the oral platelet inhibitors dipyridamole and acetylsalicylic acid is associated with increased risk of fracture

    DEFF Research Database (Denmark)

    Vestergaard, Peter; Steinberg, Thomas H; Schwarz, P

    2012-01-01

    BACKGROUND: Platelet inhibitors are widely used in the treatment and prevention of coronary artery disease. In addition to acetylsalicylic acid, two major groups of platelet inhibitors are used; phosphodiesterase inhibitors including dipyridamole, and thienopyridines (ticlopidine and clopidogrel......). Clopidogrel is the most widely used, and in combination with acetylsalicylic acid it is the standard of care for acute coronary syndromes and percutaneous coronary interventions. However, the modes of action involve pathways that are involved in the metabolic activity in bone cells and pharmacologic...... found that treatment with dipyridamole is associated with increased overall fracture risk, but not to the risk of osteoporotic fractures. In contrast, low-dose acetylsalicylic acid is associated to increased risk of overall fractures and fractures of the hip. Finally, in the current study clopidogrel...

  9. Does the use of acetylsalicylic acid have an influence on our vision?

    Directory of Open Access Journals (Sweden)

    Michalska-Małecka K

    2016-11-01

    Full Text Available Katarzyna Michalska-Małecka,1,2 Agnieszka Regucka,2 Dorota Śpiewak,2 Magdalena Sosnowska-Pońska,2 Alfred Niewiem2 1Department of Ophthalmology, School of Medicine in Katowice, Medical University of Silesia, Katowice, Poland; 2University Clinical Center, University Hospital Medical University of Silesia, Katowice, Poland Purpose: Acetylsalicylic acid (ASA is one of the most commonly used drugs in the world due to its anti-inflammatory, analgesic, and antipyretic properties. This review aims to describe the relationship between acetylsalicylic acid and age-related macular degeneration (AMD – a chronic disease that causes deterioration of visual acuity and is one of the most common ophthalmological diseases these days. Methods: Data presented in this review were collected from both research and review articles concerning ophthalmology and pharmacology. Results: The results of the studies analyzed in this review are not unambiguous. Moreover, the studies are not homogenous. They differed from one another in terms of the number of patients, the age criteria, the ASA dose, and the duration of control period. The reviewed studies revealed that ASA therapy, which is applied as a protection in cardiovascular diseases in patients with early forms of AMD and geographic atrophy, should not be discontinued. Conclusion: On the basis of the present studies, it cannot be unequivocally said whether ASA influences people’s vision and if people endangered with AMD progression or who are diagnosed with AMD should use this drug. It may increase the risk of AMD, but it can also reduce the risk of life-threatening conditions. The authors suggest that in order to avoid possible risks of AMD development, people who frequently take ASA should have their vision checked regularly. Keywords: acetylsalicylic acid, AMD, lipofuscin genesis, drusen genesis, retinal pigment epithelium cells, geographic atrophy

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

    Science.gov (United States)

    Rogić, Dunja

    1993-03-01

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

  11. DFT studies on the vibrational and electronic spectra of acetylsalicylic acid

    Science.gov (United States)

    Ye, Yunfeng; Tang, Guodong; Han, Yonghong; Culnane, Lance F.; Zhao, Jianyin; Zhang, Yu

    2016-05-01

    The following is a theoretical and experimental study on the vibrational and electronic properties of acetylsalicylic acid (ASA). Vibrational information was obtained by FT-IR and Raman spectroscopy which agree well with harmonic vibrational frequency calculations. The calculations were carried out using density functional theory B3LYP methods with 6-311G** and LANL2DZ basis sets. The vibrational assignments were calculated by Gaussview. Absorption UV-Vis experiments of ASA reveal three maximum peaks at 203, 224 and 277 nm, which are in agreement with calculated electronic transitions using TD-B3LYP/6-311G**.

  12. Protective Effect of Melatonin on the Quality of Spermatogenesis and Sperm Parameters in the Mice Treated with Acetylsalicylic Acid

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    F. Mohammad Ghasemi

    2012-01-01

    Full Text Available Introduction & Objective: Melatonin, the most important secretary hormone of pineal gland, as a powerful antioxidant has a high potent for neutralizing the toxicity of drugs. In the present study we aimed to demonstrate the effect of melatonin on testicular damage and sperm parameters deficiency induced by acetylsalicylic acid, in adult male mice. Materials & Methods: Male NMRI mice were divided into 4 groups: 1 control 2 acetylsalicylic acid treated group 3 melatonin treated group 4 Melatonin-acetylsalicylic acid treated group. Acetylsalicylic acid was administered at a dose of 50mg/kg orally through gavage for 14 days. Melatonin was administered in dose of 10 mg/kg for 5 days intraperitoneally. The control mice were received vehicle (normal saline orally through gavage. The animals were sacrificed and their testes and epididymis were dissected on the 15th day after the treatment. Evaluations were made by determining Johnson's score, epididymal sperm count, and sperm morphology and sperm motility. Statistical analysis was performed by ANOVA test. Results: Acetylsalicylic acid treated mice showed a reduction in Johnson's score and quality of spermatogenesis (P<0.05, sperm count, normal morphology and motility percent (P<0.001, compared to the control. Melatonin in group 4, significantly increased maturation of seminiferous tubules (P<0.05, and quality and quantity of sperm parameters (P<0.05 in comparison with group 2. Conclusion: It seems that intraperitoneal administration of melatonin for 5 days is a potentially beneficial agent to improve the quality of spermatogenesis and sperm parameters in testis damaged by acetylsalicylic acid, probably by decreasing oxidative stresses. (Sci J Hamadan Univ Med Sci 2012;18(4:29-36

  13. [Study of acetylsalicylic acid role in the potentiation of antiamnesic and neuroprotective properties of piracetam in rats with alloxan diabetes].

    Science.gov (United States)

    Zhiliuk, V I; Levykh, A E; Mamchur, V I

    2013-01-01

    It has been established that prolonged alloxan-induced hyperglycemia in rats potentiates amnesic properties of scopolamine hydrobromide. It was characterized by shortening of the latent period by 44% (ppiracetam with acetylsalicylic acid was accompanied by an expressed antiamnetic potential - the reduction of early markers of proteins degradation (aldehydephenylhydrazones, APH) by 21,7% (ppiracetam according to the effect upon KPH. NO2-/NO3- level was also decreased by 30,3% (ppiracetam may be assumed to be directly related to the ability of acetylsalicylic acid to improve microcirculation in the ischemic areas of the brain in diabetes and probably to its neuroprotective potential.

  14. Proton-pump inhibitor therapy for acetylsalicylic acid associated upper gastrointestinal symptoms: a randomized placebo-controlled trial.

    NARCIS (Netherlands)

    Laheij, R.J.F.; Rossum, L.G.M. van; Jansen, J.B.M.J.; Verheugt, F.W.A.

    2003-01-01

    OBJECTIVE: Patients using acetylsalicylic acid (aspirin) have an increased risk of upper gastrointestinal discomfort. The aim of this study was to assess whether gastric acid suppression improves upper gastrointestinal symptoms in patients using low-dose aspirin for cardiovascular disease. METHODS:

  15. Medications Containing Aspirin (Acetylsalicylate) and Aspirin-Like Products

    Science.gov (United States)

    ... Some medication labels may use the words acetylsalicylate, acetylsalicylic acid, salicylic, salicylamide, phenyl salicylate, etc., instead of the word aspirin. There is not data as to other forms ...

  16. IR spectroscopic investigation of the inhibition of the glycation process by acetylsalicylic acid

    Science.gov (United States)

    Otero de Joshi, Virginia; Gil, Herminia; Contreras, Silvia; Velasquez, William; Joshi, Narahari V.

    2000-05-01

    An IR spectroscopic study was carried out at room temperature for Human Serum albumin (HSA) glycated with fructose and glucose and inhibited with acetylsalicylic acid. The glycation process was carried out in our laboratory by a conventional method to confirm earlier reported observation of the effect of glycation on the intensity variation of the IR spectra, particularly, in the range 1500 cm-1 to 1700 cm-1 and around 3300 cm-1. IR spectra reveal that the effects of glycation of HSA by fructose are more intense than with glucose, which is the expected. Bovine serum albumin was also glycated using Glucose-6-phosphate disodium salt, and gamma-globulin was glycate with glucose, As expected, the glycation process was more intense with glucose-t-phosphate disodium salt. Acetyl salicylic acid was also used and its inhibitor effects could be observed in both cases, with glucose and with glucose-6-phosphate disodium salt even though, to a smaller extent with the latter. This is consistent with the earlier data and is explained on the basis of the attachment of macromolecules to (epsilon) -NH2 groups of lysines. The experimental results confirm that acetylsalicylic acid, indeed, acts as an inhibitor by acetylation of the (epsilon) -NG2 group where the sugars are supposed to be attached.

  17. Effect of O-acetylsalicylic acid on lipid synthesis by guinea pig gastric mucosa in vitro

    Energy Technology Data Exchange (ETDEWEB)

    Spohn, M.; McColl, I.

    1987-01-01

    The aim of this work was to investigate the involvement of lipids as possible components of the gastric mucosal barrier by studying the synthesis and secretion of lipids by the epithelial cell lining of gastric mucosa and the effect of salicylate on these processes. O-Acetylsalicylic acid reversibly reduced in vitro incorporation of (U-/sup 14/C) and of DL-(2-/sup 14/C) mevalonic acid into lipids by isolated epithelial cells and by intact mucosa of guinea pig stomach, indicating reversible inhibition of lipid synthesis by the tissue in the presence of the drug. Inhibition of incorporation of both precursors into total lipids, into their fatty acid components, and into cholesterol is demonstrated. 19 refs.

  18. Identification and Quantitative Analysis of Acetaminophen, Acetylsalicylic Acid, and Caffeine in Commercial Analgesic Tablets by LC-MS

    Science.gov (United States)

    Fenk, Christopher J.; Hickman, Nicole M.; Fincke, Melissa A.; Motry, Douglas H.; Lavine, Barry

    2010-01-01

    An undergraduate LC-MS experiment is described for the identification and quantitative determination of acetaminophen, acetylsalicylic acid, and caffeine in commercial analgesic tablets. This inquiry-based experimental procedure requires minimal sample preparation and provides good analytical results. Students are provided sufficient background…

  19. Numerical simulation of the solvate structures of acetylsalicylic acid in supercritical carbon dioxide containing polar co-solvents

    Science.gov (United States)

    Petrenko, V. E.; Antipova, M. L.; Gurina, D. L.; Odintsova, E. G.; Kumeev, R. S.; Golubev, V. A.

    2016-07-01

    Hydrogen-bonded complexes of acetylsalicylic acid with polar co-solvents in supercritical carbon dioxide, modified by methanol, ethanol, and acetone of 0.03 mole fraction concentration, are studied by numerical methods of classical molecular dynamics simulation and quantum chemical calculations. The structure, energy of formation, and lifetime of hydrogen-bonded complexes are determined, along with their temperature dependences (from 318 to 388 K at constant density of 0.7 g cm-3). It is shown that the hydrogen bonds between acetylsalicylic acid and methanol are most stable at 318 K and are characterized by the highest value of absolute energy. At higher supercritical temperatures, however, the longest lifetime is observed for acetylsalicylic acid-ethanol complexes. These results correlate with the known literature experimental data showing that the maximum solubility of acetylsalicylic acid at density values close to those considered in this work and at temperatures of 318 and 328 K is achieved when using methanol and ethanol as co-solvents, respectively.

  20. Pharmacokinetics and pharmacodynamics of acetylsalicylic acid after intravenous and oral administration to healthy volunteers

    Directory of Open Access Journals (Sweden)

    Nagelschmitz J

    2014-03-01

    Full Text Available J Nagelschmitz,1 M Blunck,1 J Kraetzschmar,1 M Ludwig,1 G Wensing,1 T Hohlfeld2 1Bayer HealthCare AG, Clinical Pharmacology, Wuppertal, Germany; 2Institut für Pharmakologie und Klinische Pharmakologie, Heinrich-Heine Universität Düsseldorf, Düsseldorf, Germany Background: The pharmacology of single doses of acetylsalicylic acid (ASA administered intravenously (250 or 500 mg or orally (100, 300, or 500 mg was evaluated in a randomized, placebo-controlled, crossover study. Methods: Blood and urine samples were collected before and up to 24 hours after administration of ASA in 22 healthy volunteers. Pharmacokinetic parameters and measurements of platelet aggregation were determined using validated techniques. Results: A comparison between administration routes showed that the geometric mean dose-corrected peak concentrations (Cmax/D and the geometric mean dose-corrected area under the curve (AUC0–∞/D were higher following intravenous administration of ASA 500 mg compared with oral administration (estimated ratios were 11.23 and 2.03, respectively. Complete inhibition of platelet aggregation was achieved within 5 minutes with both intravenous ASA doses, reflecting a rapid onset of inhibition that was not observed with oral dosing. At 5 minutes after administration, the mean reduction in arachidonic acid-induced thromboxane B2 synthesis ex vivo was 99.3% with ASA 250 mg intravenously and 99.7% with ASA 500 mg intravenously. In exploratory analyses, thromboxane B2 synthesis was significantly lower after intravenous versus oral ASA 500 mg (P<0.0001 at each observed time point up to the first hour after administration. Concentrations of 6-keto-prostaglandin1α at 5 and 20 minutes after dosing were also significantly lower with ASA 500 mg intravenously than with ASA 500 mg orally. Conclusion: This study demonstrates that intravenous ASA provides more rapid and consistent platelet inhibition than oral ASA within the first hour after dosing

  1. Using Capillary Electrophoresis to Determine the Purity of Acetylsalicylic Acid Synthesized in the Undergraduate Laboratory

    Science.gov (United States)

    Welder, Frank; Colyer, Christa L.

    2001-11-01

    Capillary electrophoresis (CE), although a powerful analytical tool, has found only limited application in undergraduate laboratory study. In an effort to expose freshman and sophomore chemistry students to this technique, thereby giving them practical instrumental experience early in their careers, we propose to use CE in the analysis of student-synthesized acetylsalicylic acid (ASA). The synthesis of ASA from salicylic acid (SA) is a routine undergraduate laboratory, although students rarely have the opportunity to test the purity of their product. The CE method described herein provides students with a method to test purity and yield of their product and to determine the effect of aging on their sample. CE can accomplish this in a short period of time, with minimal disruption to the regular laboratory curriculum. Optimized separation conditions, limits of detection, and linear range for ASA and SA are also given.

  2. Quality and antioxidant properties on sweet cherries as affected by preharvest salicylic and acetylsalicylic acids treatments.

    Science.gov (United States)

    Giménez, María José; Valverde, Juan Miguel; Valero, Daniel; Guillén, Fabián; Martínez-Romero, Domingo; Serrano, María; Castillo, Salvador

    2014-10-01

    The effects of salicylic acid (SA) or acetylsalicylic acid (ASA) treatments during on-tree cherry growth and ripening on fruit quality attributes, especially those related with the content on bioactive compounds and antioxidant activity were analysed in this research. For this purpose, two sweet cherry cultivars, 'Sweet Heart' and 'Sweet Late', were used and SA or ASA treatments, at 0.5, 1.0 and 2.0mM concentrations, were applied at three key points of fruit development (pit hardening, initial colour changes and onset of ripening). These treatments increased fruit weight and ameliorated quality attributes at commercial harvest, and led to cherries with higher concentration in total phenolics and in total anthocyanins, as well as higher antioxidant activity, in both hydrophilic and lipophilic fractions. Thus, preharvest treatments with SA or ASA could be promising tools to improve sweet cherry quality and health beneficial effects for consumers.

  3. Demonstration of the analgesic efficacy and dose-response of acetylsalicylic acid with pseudoephedrine.

    Science.gov (United States)

    Schachtel, Bernard P; Voelker, Michael; Sanner, Kathleen M; Gagney, Diana; Bey, Mary; Schachtel, Emily J; Becka, Michael

    2010-12-01

    To determine acute analgesia by acetylsalicylic acid (ASA) when combined with pseudoephedrine (PSE) in patients with upper respiratory tract infection (URTI), we used the sore throat pain model to measure single-dose effects of ASA 500 mg/PSE 30 mg, ASA 1000 mg/PSE 60 mg, and acetaminophen (APAP) 1000 mg/PSE 60 mg (serving as a positive control). Under double-blind, randomized, placebo-controlled conditions, 640 adult patients with confirmed acute pharyngitis and rhinosinusitis associated with URTI rated throat pain intensity and relief at intervals over 6 hours. Efficacy was demonstrated for both doses of ASA/PSE compared with placebo for all end points, including total pain relief and summed pain intensity differences, beginning at 20 minutes on both scales (all P pseudoephedrine.

  4. Synthesis, characterisation and biological evaluation of copper and silver complexes based on acetylsalicylic acid.

    Science.gov (United States)

    Rubner, Gerhard; Bensdorf, Kerstin; Wellner, Anja; Bergemann, Silke; Gust, Ronald

    2011-10-01

    Metalcarbonyl complexes with ligands derived from acetylsalicylic acid demonstrated high cytotoxic potential against various tumor cell lines and strong inhibition of the cyclooxygenase enzymes COX-1 and 2. In this study we tried to achieve comparable effects with [alkyne]silver or copper trifluoromethanesulfonate complexes which are more hydrophilic then the uncharged metalcarbonyl derivatives. All compounds were evaluated for growth inhibition against breast (MCF-7, MDA-MB 231) and colon cancer (HT-29) cell lines and for COX-1 and COX-2 inhibitory effects at isolated isoenzymes. Pure ligands showed neither cytotoxic nor COX-inhibitory effects. While the silver complexes of (but-2-ynyl)-2-acetoxybenzoate (But-ASS-Ag) and (but-2-yne-1,4-diyl)-bis(2-acetoxybenzoate) (Di-ASS-But-Ag) were strong cytostatics, only the copper complex Di-ASS-But-Cu was active. At the COX enzymes the complexes were more effective than their ligands and aspirin.

  5. Chemometrical exploration of an isotopic ratio data set of acetylsalicylic acid

    Energy Technology Data Exchange (ETDEWEB)

    Stanimirova, I. [ChemoAC, FABI, Analytical Chemistry and Pharmaceutical Technology, Vrije Universiteit Brussel-VUB, Laarbeeklaan 103, B-1090 Brussels (Belgium); Daszykowski, M. [ChemoAC, FABI, Analytical Chemistry and Pharmaceutical Technology, Vrije Universiteit Brussel-VUB, Laarbeeklaan 103, B-1090 Brussels (Belgium); Van Gyseghem, E. [Eurofins Scientific Analytics, Rue Pierre Adolphe Bobierre, 44323 Nantes Cedex 3 (France); Bensaid, F.F. [Eurofins Scientific Analytics, Rue Pierre Adolphe Bobierre, 44323 Nantes Cedex 3 (France); Lees, M. [Eurofins Scientific Analytics, Rue Pierre Adolphe Bobierre, 44323 Nantes Cedex 3 (France); Smeyers-Verbeke, J. [ChemoAC, FABI, Analytical Chemistry and Pharmaceutical Technology, Vrije Universiteit Brussel-VUB, Laarbeeklaan 103, B-1090 Brussels (Belgium); Massart, D.L. [ChemoAC, FABI, Analytical Chemistry and Pharmaceutical Technology, Vrije Universiteit Brussel-VUB, Laarbeeklaan 103, B-1090 Brussels (Belgium); Vander Heyden, Y. [ChemoAC, FABI, Analytical Chemistry and Pharmaceutical Technology, Vrije Universiteit Brussel-VUB, Laarbeeklaan 103, B-1090 Brussels (Belgium)]. E-mail: yvanvdh@vub.ac.be

    2005-11-03

    A data set consisting of fourteen isotopic ratios or quantities derived from such ratios for samples of acetylsalicylic acid (aspirin), commercialized by various pharmaceutical companies from different countries, was analyzed. The goal of the data analysis was to explore whether results can be linked to geographical origin or other features such as different manufacturing processes, of the samples. The methods of data analysis used were principal component analysis (PCA), robust principal component analysis (RPCA), projection pursuit (PP) and multiple factor analysis (MFA). The results do not seem to depend on geographic origin, except for some samples from India. They do depend on the pharmaceutical companies. Moreover, it seems that the samples from certain pharmaceutical companies form clusters of similar samples, suggesting that there is some common feature between those pharmaceutical companies. Variable selection performed by means of MFA showed that the number of variables can be reduced to five without loss of information.

  6. GASTROENTEROPATHIES ASSOCIATED WITH ACETYLSALICYLIC ACID: HOW TO IMPROVE SAFETY OF THERAPY

    Directory of Open Access Journals (Sweden)

    A. L. Komarov

    2016-01-01

    Full Text Available Lesion of gastrointestinal mucous coat is the main factor limited acetylsalicylic acid (ASA use in patients with atherothrombosis. Up to date the mostly comprehensible way to decrease gastrointestinal complications is taking ASA in the lowest effective dose, which is not higher than 75-81 mg daily. It is necessary if possible to avoid ASK usage in combination with other antiaggregants, anticoagulants, non-steroid and steroid anti-inflammatory drugs. Routine antiulcer therapy is not indicated for patients treated with ASA because there is a lack of clinical research data about efficacy of this approach. In high risk of dangerous gastrointestinal complications H. pylori eradication is recommended in combination with long term preventive therapy with gastric secretion inhibitors. Proton pump inhibitors are more preferred.

  7. GASTROENTEROPATHIES ASSOCIATED WITH ACETYLSALICYLIC ACID: HOW TO IMPROVE SAFETY OF THERAPY

    Directory of Open Access Journals (Sweden)

    A. L. Komarov

    2009-01-01

    Full Text Available Lesion of gastrointestinal mucous coat is the main factor limited acetylsalicylic acid (ASA use in patients with atherothrombosis. Up to date the mostly comprehensible way to decrease gastrointestinal complications is taking ASA in the lowest effective dose, which is not higher than 75-81 mg daily. It is necessary if possible to avoid ASK usage in combination with other antiaggregants, anticoagulants, non-steroid and steroid anti-inflammatory drugs. Routine antiulcer therapy is not indicated for patients treated with ASA because there is a lack of clinical research data about efficacy of this approach. In high risk of dangerous gastrointestinal complications H. pylori eradication is recommended in combination with long term preventive therapy with gastric secretion inhibitors. Proton pump inhibitors are more preferred.

  8. Origin of the low temperature excess heat capacity of isotopically substituted acetylsalicylic acid

    Science.gov (United States)

    Schröder, F.; Winkler, B.; Bauer, J. D.; Haussühl, E.; Rivera Escoto, B.; Tristan López, F.; Avalos Borja, M.; Richter, C.; Ferner, J.

    2011-09-01

    The low temperature heat capacities of single crystals of fully protonated acetylsalicylic acid, measured between 2 K < T < 80 K, have been compared to samples in which the methyl-group was replaced by CD3, CH2D and 13CH3. For the partially methyl-deuterated crystal (CH2D) a significant excess heat capacity was found below T < 40 K with a broad maximum around T ≈ 14 K. The thermodynamic data are explained on the basis of a Schottky model using results obtained in earlier NMR and neutron spectroscopic experiments. In contrast, the excess heat capacity of the fully deuterated compound can be explained by a change of the phonon density of states.

  9. Drug delivery and therapeutic impact of extended-release acetylsalicylic acid.

    Science.gov (United States)

    Bliden, Kevin P; Patrick, Jeff; Pennell, Andrew T; Tantry, Udaya S; Gurbel, Paul A

    2016-01-01

    Current treatment guidelines recommend once-daily, low-dose acetylsalicylic acid (ASA; aspirin) for secondary prevention of cardiovascular events. However, the anti-thrombotic benefits of traditional ASA formulations may not extend over a 24-h period, especially in patients at high risk for a recurrent cardiovascular event. A next-generation, extended-release ASA formulation (ER-ASA) has been developed to provide 24-h anti-thrombotic coverage with once-daily dosing. The pharmacokinetics of ER-ASA indicates slower absorption and prolonged ASA release versus immediate-release ASA, with a favorable safety profile. ER-ASA minimizes systemic ASA absorption and provides sustained antiplatelet effects over a 24-h period.

  10. Controlled release of acetylsalicylic acid from polythiophene/carrageenan hydrogel via electrical stimulation.

    Science.gov (United States)

    Pairatwachapun, Sanita; Paradee, Nophawan; Sirivat, Anuvat

    2016-02-10

    Blends between polythiophene (PTh) and a carrageenan hydrogel were fabricated as the matrix for the electric field assisted drug release. The pristine carrageenan and the blend films were prepared by the solution casting using acetylsalicylic acid (ASA) as the anionic model drug and Mg(2+), Ca(2+), and Ba(2+) as the crosslinking agents. The ASA was released by the Fickian diffusion mechanism. The diffusion coefficient decreased with increasing crosslinking ratio or decreasing crosslinking ionic radii. The diffusion coefficients were greater with the applied electrical potentials by an order of magnitude relative to those without electric field. Moreover, the diffusion coefficients with PTh as the drug carrier were higher than those without PTh. Thus, the presence of the conductive polymer in the hydrogel blend coupled with applied electric field is shown here to drastically enhance the drug delivery rate.

  11. The effect of acetylsalicylic acid and meloxicamon hematological parameters in rats

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    Ćupić Vitomir

    2015-01-01

    Full Text Available In this work there was investigated the effect of two nonsteroidal antiinflammatory drugs (NSAIDs, acetylsalicylic acid or aspirin (nonselective cyclooxygenase inhibitor - COX1 i COX2 and meloxicam (selective cyclooxygenase inhibitor - COX2 on certain hematological parameters in rats. The objective of the work was to determine whether (and to which extent, these drugs, after multiple peroral application, influence erythrocyte number, concentration of hemoglobin, hematological indices (mean corpuscular value - MCV; mean concentration of hemoglobin in erythrocytes - MCH; mean corpuscular hemoglobin concentration - MCHC, hematocrit, number of platelets, leukocytes, neutrophilic leukocytes, lymphocytes and monocytes. The experiment was conducted in in vivo conditions on 70 clinically healthy Wistar strain male rats, 10 to 12 weeks of age and body weight 250 to 300 g. The rats were divided into seven groups and they were daily perorally (by probe given aspirin (ASCOPIR at doses of 30, 40 and 80 mg/kg b.m. (I, II and III groups, or meloxicam (METACAM at doses of 100, 125 and 250 μg/kg b.m. (IV, V and VI groups, for seven days. The seventh group was a control one and they were given only saline. The obtained results showed that: acetylsalicylic acid in maximum dose tested (80 mg/kg b.m. statistically significantly reduced the number of platelets (p<0,05, the number of leukocytes (p<0,05, the number of lymphocytes (p<0,05 and the number of monocytes (p<0,05, while on the other side, meloxicam in maximum dose tested (250 μg/kg, statistically significantly reduced the mean corpuscular value (MCV, and increased the number of platelets (p<0,05, relative to the control value.

  12. Thermodynamics of inclusion complexes of natural and modified cyclodextrins with acetylsalicylic acid and ibuprofen in aqueous solution at 298 K

    Energy Technology Data Exchange (ETDEWEB)

    Castronuovo, Giuseppina, E-mail: giuseppina.castronuovo@unina.it [Department of Chemistry, University Federico II of Naples, Complesso Universitario a Monte S. Angelo, via Cintia, 80126 Naples (Italy); Niccoli, Marcella [Department of Chemistry, University Federico II of Naples, Complesso Universitario a Monte S. Angelo, via Cintia, 80126 Naples (Italy)

    2013-04-10

    Graphical abstract: Complexation forces acting in the association between natural and modified α- and β-cyclodextrins and acetylsalicylic acid (aspirin) or ibuprofen are examined through the analysis of the thermodynamic parameters obtained by isothermal calorimetry. Highlights: ► A calorimetric method is reported to study the association of natural and substituted cyclodextrins with acetylsalicylic acid and ibuprofen. ► The study aims to propose a hypothesis about the forces involved in the interaction. That can be useful for designing new cyclodextrins having suitable characteristics to include specific drugs. ► Enthalpic and entropic contributions on the association are discussed. The differences in the cavity dimensions of the cyclodextrins determine the values of the thermodynamic properties to be very different. - Abstract: Thermodynamic parameters for the association of natural and substituted α-, β-, and γ-cyclodextrins with acetylsalicylic acid, salicylic acid and ibuprofen have been determined by isothermal titration calorimetry. Analysis of the data shows that complexes form, all having 1:1 stoichiometry. The shape-matching between the host and guest is the factor determining the values of the thermodynamic quantities. In the case of the smallest cyclodextrin interacting with acetylsalicylic acid and salicylic acid, the parameters indicate that hydrophobic interactions play the major role. Association occurs through the shallow inclusion of the benzene ring into the cavity. In the case of substituted β-cyclodextrins, instead, inclusion of the benzene ring is deeper and the tight fitting of the guest molecule to the cavity makes the enthalpy and entropy to be both negative. Ibuprofen interacts through its isobutyl group: the values of the association constants are very high for β-cyclodextrins as determined by the large and positive entropies due to the relaxation of water molecules from the cavity and the hydration spheres of the interacting

  13. Effects of acetylsalicylic acid on fresh weight pigment and protein content of bean leaf discs (Phaseolus vulgaris L.).

    Science.gov (United States)

    Canakçi, S

    2003-01-01

    The effects of 100, 250, and 500 ppm acetylsalicylic acid solutions treatments on weight alteration, pigment and protein amounts in discs from the primary leaves of one month old bean (Phaseolus vulgaris L.) seedlings produced tinder greenhouse conditions are presented. The experiments show that: 100 ppm ASA had no significant influence (P > 0.05) but 250 and 500 ppm ASA caused an increase on weight loss (P 0.05), none of the ASA treatments caused a statistically significant influence on carotenoid amount (P > 0.05); 100 and 250 ppm ASA treatments did not cause a significant influence on protein amount (P > 0.05). however 500 ppm ASA treatment caused an increase on protein injury (P < 0.05). Consequently, it is supposed that wet weight loss, pigment and protein injury have somewhat increased on leaf discs. depending on the toxic effect of high acetylsalicylic acid concentrations.

  14. Protective effects of electroacupuncture on acetylsalicylic acid-induced acute gastritis in rats

    Institute of Scientific and Technical Information of China (English)

    Hye Suk Hwang; Kyung-Ju Han; Yeon Hee Ryu; Eun Jin Yang; Yoo Sung Kim; Sang Yong Jeong; Young-Seop Lee; Myeong Soo Lee; Sung Tae Koo; Sun-Mi Choi

    2009-01-01

    AIM: To invest igate the protect ive effects of electroacupuncture (EA) pretreatment on acetylsalicylic acid (ASA)-induced ulceration in rats. METHODS: We randomly divided 72 rats into three groups including control (administered with distilled water), ASA group (administered 100 mg/kg ASA) and EA group (administered EA + 100 mg/kg ASA). Each rat was fasted for 18 to 24 h before experimentation, and lesion scores, gastric acidity, cyclooxygenase (COX)-1 and -2 mRNA levels, and total nitric oxide (NO) concentration were measured. RESULTS: The lesion scores of the EA group were significantly lower than those of the ASA group. Gastric acidity of the ASA and EA groups was reduced compared to the control group. COX-1 and -2 mRNA levels were significantly increased in the EA group as compared to the control and ASA groups, and NO levels were also significantly increased in the EA group as compared to the ASA group. CONCLUSION: These results suggest that EAmediated protection against ASA-induced ulceration in rats may occur via gastric defense components.

  15. Effect of tocopherol and acetylsalicylic acid on the biochemical indices of blood in dioxin-exposed rats.

    Science.gov (United States)

    Rosińczuk, Joanna; Całkosiński, Ireneusz

    2015-07-01

    New sources of dioxins and increased dioxin concentrations in the environment, coupled with their increased bioavailability along the food chain and accumulation in adipose tissues, contribute to various adverse long-term biological effects. The purpose of the study was to determine whether tocopherol protects the CNS by decreasing the pro-inflammatory influence of free radicals generated by TCDD; whether acetylsalicylic acid inhibits the production of inflammatory mediators; and whether the combined administration of tocopherol and acetylsalicylic acid to TCDD-exposed rats has a potential CNS-protective effect. The study included 117 rats divided into 8 groups: 75 female and 12 male Buffalo rats aged 8-10 weeks, weighing 140-160 g; as well as 30 female rats aged 6 weeks and weighing 120 g, which were the offspring of females from each study group. In the experiment, the following substances were used: 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD), dosed at 5 μg/kg BW and 12.5 μg/kg BW, diluted in a 1% DMSO solution at the concentration of 1 μg/ml; α-tocopherol acetate, dosed at 30 mg/kg BW, in 0.2 ml of oil solution; and acetylsalicylic acid, 50mg/kg BW, suspended in 0.5 ml of starch solution, administered orally using a feeding tube. Pleurisy was induced by an injection of 0.15 ml of 1% carrageenin solution. The use of tocopherol reduces the adverse effects of the inflammatory reaction induced by TCDD. Administering tocopherol improves protein metabolism by reducing protein catabolism, and raises γ-globulin fraction levels. Combined acetylsalicylic acid and tocopherol suppress catabolic processes accompanying inflammation.

  16. Acetylsalicylic acid regulates MMP-2 activity and inhibits colorectal invasion of murine B16F0 melanoma cells in C57BL/6J mice: effects of prostaglandin F(2)alpha.

    Science.gov (United States)

    Tsai, Chin-Shaw Stella; Luo, Shue-Fen; Ning, Chung-Chu; Lin, Chien-Liang; Jiang, Ming-Chung; Liao, Ching-Fong

    2009-08-01

    Epidemiological studies indicate that acetylsalicylic acid may reduce the risk of mortality due to colon cancers. Metastasis is the major cause of cancer death. Matrix metalloproteinases (MMPs) play important roles in tumor invasion regulation, and prostaglandin F(2)alpha (PGF(2)alpha) is a key stimulator of MMP production. Thus, we investigated whether acetylsalicylic acid regulated MMP activity and the invasion of cancer cells and whether PGF(2)alpha attenuated acetylsalicylic acid-inhibited invasion of cancer cells. Gelatin-based zymography assays showed that acetylsalicylic acid inhibited the MMP-2 activity of B16F0 melanoma cells. Matrigel-based chemoinvasion assays showed that acetylsalicylic acid inhibited the invasion of B16F0 cells. Acetylsalicylic acid can inhibit PGF(2)alpha synthesis and PGF(2)alpha is a key stimulator of MMP-2 production. Our data showed that PGF(2)alpha treatment attenuated the acetylsalicylic acid-inhibited invasion of B16F0 cells. In animal experiments, acetylsalicylic acid reduced colorectal metastasis of B16F0 cells in C57BL/6J mice by 44%. Our results suggest that PGF(2)alpha is a therapeutic target for metastasis inhibition and acetylsalicylic acid may possess anti-metastasis ability.

  17. Local sustained delivery of acetylsalicylic acid via hybrid stent with biodegradable nanofibers reduces adhesion of blood cells and promotes reendothelialization of the denuded artery.

    Science.gov (United States)

    Lee, Cheng-Hung; Lin, Yu-Huang; Chang, Shang-Hung; Tai, Chun-Der; Liu, Shih-Jung; Chu, Yen; Wang, Chao-Jan; Hsu, Ming-Yi; Chang, Hung; Chang, Gwo-Jyh; Hung, Kuo-Chun; Hsieh, Ming-Jer; Lin, Fen-Chiung; Hsieh, I-Chang; Wen, Ming-Shien; Huang, Yenlin

    2014-01-01

    Incomplete endothelialization, blood cell adhesion to vascular stents, and inflammation of arteries can result in acute stent thromboses. The systemic administration of acetylsalicylic acid decreases endothelial dysfunction, potentially reducing thrombus, enhancing vasodilatation, and inhibiting the progression of atherosclerosis; but, this is weakened by upper gastrointestinal bleeding. This study proposes a hybrid stent with biodegradable nanofibers, for the local, sustained delivery of acetylsalicylic acid to injured artery walls. Biodegradable nanofibers are prepared by first dissolving poly(D,L)-lactide-co-glycolide and acetylsalicylic acid in 1,1,1,3,3,3-hexafluoro-2-propanol. The solution is then electrospun into nanofibrous tubes, which are then mounted onto commercially available bare-metal stents. In vitro release rates of pharmaceuticals from nanofibers are characterized using an elution method, and a highperformance liquid chromatography assay. The experimental results suggest that biodegradable nanofibers release high concentrations of acetylsalicylic acid for three weeks. The in vivo efficacy of local delivery of acetylsalicylic acid in reducing platelet and monocyte adhesion, and the minimum tissue inflammatory reaction caused by the hybrid stents in treating denuded rabbit arteries, are documented. The proposed hybrid stent, with biodegradable acetylsalicylic acid-loaded nanofibers, substantially contributed to local, sustained delivery of drugs to promote re-endothelialization and reduce thrombogenicity in the injured artery. The stents may have potential applications in the local delivery of cardiovascular drugs. Furthermore, the use of hybrid stents with acetylsalicylic acid-loaded nanofibers that have high drug loadings may provide insight into the treatment of patients with high risk of acute stent thromboses.

  18. Biowaiver monograph for immediate-release solid oral dosage forms: acetylsalicylic acid.

    Science.gov (United States)

    Dressman, Jennifer B; Nair, Anita; Abrahamsson, Bertil; Barends, Dirk M; Groot, D W; Kopp, Sabine; Langguth, Peter; Polli, James E; Shah, Vinod P; Zimmer, Markus

    2012-08-01

    A biowaiver monograph for acetylsalicylic acid (ASA) is presented. Literature and experimental data indicate that ASA is a highly soluble and highly permeable drug, leading to assignment of this active pharmaceutical ingredient (API) to Class I of the Biopharmaceutics Classification System (BCS). Limited bioequivalence (BE) studies reported in the literature indicate that products that have been tested are bioequivalent. Most of the excipients used in products with a marketing authorization in Europe are not considered to have an impact on gastrointestinal motility or permeability. Furthermore, ASA has a wide therapeutic index. Thus, the risks to the patient that might occur if a nonbioequivalent product were to be incorrectly deemed bioequivalent according to the biowaiver procedure appear to be minimal. As a result, the BCS-based biowaiver procedure can be recommended for approval of new formulations of solid oral dosage forms containing ASA as the only API, including both multisource and reformulated products, under the following conditions: (1) excipients are chosen from those used in ASA products already registered in International Conference on Harmonization and associated countries and (2) the dissolution profiles of the test and the comparator products comply with the BE guidance.

  19. The study of acetylsalicylic acid effects on wheat seeds germination in salt stress conditions

    Directory of Open Access Journals (Sweden)

    Sorin Tănasa

    2010-12-01

    Full Text Available The present study was conducted in order to determine whether a treatment using acetylsalicylic acid (ASA would increase the germinative energy of wheat seeds in conditions of salt stress. Wheat seeds were immersed in six solutions of ASA of different concentrations (0, 0.1, 0.5, 1, 2 and 3 mM and then germinated in two solutions of different levels of salinity (one replicating normal conditions of salinity in crop soils, and one reproducing the conditions present in salty soil. The optimum concentration ofASA for alleviating the effects of salt stress proved to be 1 mM. The enzymatic activities of three antioxidant enzymes (catalase, peroxidase and poliphenoloxidase were also monitored in all theexperimental variants to determine whether the effects of the ASA on wheat seeds germination were due to its effects on the antioxidant system. The treatment using ASA in 1 mM concentration increased,in high salinity conditions, foremost the catalase activity and less the peroxidase and poliphenoloxidase activity, making catalase the most indicative enzyme in explaining the effects of ASA on saline stress reduction.

  20. Low-dose acetylsalicylic acid and bleeding risks with ventriculoperitoneal shunt placement.

    Science.gov (United States)

    Kamenova, Maria; Croci, Davide; Guzman, Raphael; Mariani, Luigi; Soleman, Jehuda

    2016-09-01

    OBJECTIVE Ventriculoperitoneal (VP) shunt placement is a common procedure for the treatment of hydrocephalus following diverse neurosurgical conditions. Most of the patients present with other comorbidities and receive antiplatelet therapy, usually acetylsalicylic acid (ASA). Despite its clinical relevance, the perioperative management of these patients has not been sufficiently investigated. The aim of this study was to compare the peri- and postoperative bleeding complication rates associated with ASA intake in patients undergoing VP shunt placement. METHODS Of 172 consecutive patients undergoing VP shunt placement between June 2009 and December 2015, 40 (23.3%) patients were receiving low-dose ASA treatment. The primary outcome measure was bleeding events in ASA users versus nonusers, whereas secondary outcome measures were postoperative cardiovascular events, hematological findings, morbidity, and mortality. A subgroup analysis was conducted in patients who discontinued ASA treatment for < 7 days (n = 4, ASA Group 1) and for ≥ 7 days (n = 36, ASA Group 2). RESULTS No statistically significant difference for bleeding events was observed between ASA users and nonusers (p = 0.30). Cardiovascular complications, surgical morbidity, and mortality did not differ significantly between the groups either. Moreover, there was no association between ASA discontinuation regimens (< 7 days and ≥ 7 days) and hemorrhagic events. CONCLUSIONS Given the lack of guidelines regarding perioperative management of neurosurgical patients with antiplatelet therapy, these findings elucidate one issue, showing comparable bleeding rates in ASA users and nonusers undergoing VP shunt placement.

  1. Effects of Acetylsalicylic Acid Usage on Inflammatory and Oxidative Stress Markers in Hemodialysis Patients.

    Science.gov (United States)

    Maniglia, Fabíola Pansani; da Costa, José Abrão Cardeal

    2016-02-01

    The aims of this study were to determine the effects of acetylsalicylic acid (ASA) on inflammation and oxidative stress markers in hemodialysis (HD) patients and to examine the associations between these markers and the sociodemographic and clinical characteristics of participants. The study included 36 subjects who used 300 mg of ASA for 60 days. Inflammation and oxidative stress were assessed based on levels of biochemical markers. ASA usage promoted a decrease in high-sensitivity C-reactive protein (p = 0.01). The level of hydrogen peroxide increased after 30 days of use of ASA and subsequently decreased (p = 0.01). Reduced glutathione reduced at the end of the study (p < 0.01); the malondialdehyde level did not change and the levels of vitamins A and E were inverse to drug use (p = 0.01). ASA usage promoted reduced levels of inflammation, increased production of markers of oxidative stress, and reduced antioxidant defense.

  2. Dual effects of acetylsalicylic acid on ERK signaling and Mitf transcription lead to inhibition of melanogenesis.

    Science.gov (United States)

    Nishio, Takashi; Usami, Mai; Awaji, Mizuki; Shinohara, Sumire; Sato, Kazuomi

    2016-01-01

    Acetylsalicylic acid (ASA) is widely used as an analgesic/antipyretic drug. It exhibits a wide range of biological effects, including preventative effects against heart attack and stroke, and the induction of apoptosis in various cancer cells. We previously found that ASA inhibits melanogenesis in B16 melanoma cells. However, the mechanisms of how ASA down-regulates melanin synthesis remain unclear. Here, we investigated the effect of ASA on melanogenic pathways, such as extracellular signal-regulated kinase (ERK) and microphthalmia-associated transcription factor (Mitf) transcription. ASA significantly inhibited melanin synthesis in a dose-dependent manner without oxidative stress and cell death. Semi-quantitative reverse transcription-polymerase chain reaction analysis showed that the inhibitory effect of ASA might be due to the inhibition of Mitf gene transcription. Interestingly, ASA also induced ERK phosphorylation. Additionally, treatment with PD98059, a specific ERK phosphorylation inhibitor, abolished the anti-melanogenic effect of ASA. These results suggest that the depigmenting effect of ASA results from down-regulation of Mitf, which is induced by both the induction of ERK phosphorylation and the inhibition of Mitf transcription.

  3. Effects of caffeine and paracetamol alone or in combination with acetylsalicylic acid on prostaglandin E(2) synthesis in rat microglial cells.

    Science.gov (United States)

    Fiebich, B L; Lieb, K; Hüll, M; Aicher, B; van Ryn, J; Pairet, M; Engelhardt, G

    2000-08-23

    Paracetamol has mild analgesic and antipyretic properties and is, along with acetylsalicylic acid, one of the most popular "over the counter" analgesic agents. However, the mechanism underlying its clinical effects is unknown. Another drug whose mechanism of action is unknown is caffeine, which is often used in combination with other analgesics, augmenting their effect. We investigated the inhibitory effect of paracetamol and caffeine on lipopolysaccharide (LPS)-induced cyclooxygenase (COX)- and prostaglandin (PG)E(2)-synthesis in primary rat microglial cells and compared it with the effect of acetylsalicylic acid, salicylic acid, and dipyrone. Furthermore, combinations of these drugs were used to investigate a possible synergistic inhibitory effect on PGE(2)-synthesis. Both paracetamol (IC(50)=7.45 microM) and caffeine (IC(50)=42.5 microM) dose-dependently inhibited microglial PGE(2) synthesis. In combination with acetylsalicylic acid (IC(50)=3.12 microM), both substances augmented the inhibitory effect of acetylsalicylic acid on LPS-induced PGE(2)-synthesis. Whereas paracetamol inhibited only COX enzyme activity, caffeine also inhibited COX-2 protein synthesis. These results are compatible with the view that the clinical activity of paracetamol and caffeine is due to inhibition of COX. Furthermore, these results may help explain the clinical experience of an adjuvant analgesic effect of caffeine and paracetamol when combined with acetylsalicylic acid.

  4. Water-soluble nitric-oxide-releasing acetylsalicylic acid (ASA) prodrugs.

    Science.gov (United States)

    Rolando, Barbara; Lazzarato, Loretta; Donnola, Monica; Marini, Elisabetta; Joseph, Sony; Morini, Giuseppina; Pozzoli, Cristina; Fruttero, Roberta; Gasco, Alberto

    2013-07-01

    A series of water-soluble (benzoyloxy)methyl esters of acetylsalicylic acid (ASA), commonly known as aspirin, are described. The new derivatives each have alkyl chains containing a nitric oxide (NO)-releasing nitrooxy group and a solubilizing moiety bonded to the benzoyl ring. The compounds were synthesized and evaluated as ASA prodrugs. After conversion to the appropriate salt, most of the derivatives are solid at room temperature and all possess good water solubility. They are quite stable in acid solution (pH 1) and less stable at physiological pH. In human serum, these compounds are immediately metabolized by esterases, producing a mixture of ASA, salicylic acid (SA), and of the related NO-donor benzoic acids, along with other minor products. Due to ASA release, the prodrugs are capable of inhibiting collagen-induced platelet aggregation of human platelet-rich plasma. Simple NO-donor benzoic acids 3-hydroxy-4-(3-nitrooxypropoxy)benzoic acid (28) and 3-(morpholin-4-ylmethyl)-4-[3-(nitrooxy)propoxy]benzoic acid (48) were also studied as representative models of the whole class of benzoic acids formed following metabolism of the prodrugs in serum. These simplified derivatives did not trigger antiaggregatory activity when tested at 300 μM. Only 28 displays quite potent NO-dependent vasodilatatory action. Further in vivo evaluation of two selected prodrugs, {[2-(acetyloxy)benzoyl]oxy}methyl-3-[(3-[aminopropanoyl)oxy]-4-[3-(nitrooxy)propoxy]benzoate⋅HCl (38) and {[2-(acetyloxy)benzoyl]oxy}methyl 3-(morpholin-4-ylmethyl)-4-[3-(nitrooxy)propoxy]benzoate oxalate (49), revealed that their anti-inflammatory activities are similar to that of ASA when tested in the carrageenan-induced paw edema assay in rats. The gastrotoxicity of the two prodrugs was also determined to be lower than that of ASA in a lesion model in rats. Taken together, these results indicated that these NO-donor ASA prodrugs warrant further investigation for clinical application.

  5. Development and validation of a liquid chromatographic method for purity control of clopidogrel-acetylsalicylic acid in combined oral dosage forms.

    Science.gov (United States)

    Kahsay, Getu; Van Schepdael, Ann; Adams, Erwin

    2012-03-05

    A reversed phase liquid chromatographic method with UV detection for the simultaneous determination of clopidogrel and acetylsalicylic acid and their related substances in combined oral formulations was developed and validated. Good separation was achieved on a Luna C18 column (150 mm × 4.6 mm, 3 μm) using gradient elution at a flow rate of 1 mL/min and a column temperature of 35 °C. UV detection was performed at 220 nm. The validation was performed according to the ICH guidelines. The method proved to be specific, sensitive (LOQ=0.975 μg/mL and 0.0384 μg/mL for clopidogrel and acetylsalicylic acid, respectively), linear in the concentration range from LOQ to 325 μg/mL for clopidogrel and from LOQ to 650 μg/mL for acetylsalicylic acid, precise (RSD values for intermediate precision acetylsalicylic acid, respectively. Moreover, the solution stability and method robustness were examined. The method gives satisfactory separation of impurities of clopidogrel and acetylsalicylic acid and so it is suitable for quantification of the related substances as well as for the assay of the actives.

  6. Acetylsalicylic acid provides cerebrovascular protection from oxidant damage in salt-loaded stroke-prone rats.

    Science.gov (United States)

    Ishizuka, Toshiaki; Niwa, Atsuko; Tabuchi, Masaki; Ooshima, Kana; Higashino, Hideaki

    2008-03-26

    Inflammatory processes may play a pivotal role in the pathogenesis of cerebrovascular injury in salt-loaded stroke-prone spontaneously hypertensive rats (SHRSP). Recent reports revealed that acetylsalicylic acid (aspirin) has anti-oxidative properties and elicits nitric oxide release by a direct activation of the endothelial NO synthase. The present study was designed to determine whether low-dose aspirin might prevent cerebrovascular injury in salt-loaded SHRSP by protecting oxidative damage. Nine-week-old SHRSP were fed a 0.4% NaCl or a 4% NaCl diet with or without treatment by naproxen (20 mg/kg/day), salicylic acid (5 mg/kg/day), or aspirin (5 mg/kg/day) for 5 weeks. Blood pressure, blood brain barrier impairment, mortality, and the parameters of cerebrovascular inflammation and damage were compared among them. High salt intake in SHRSP significantly increased blood brain barrier impairment and early mortality, which were suppressed by treatment with aspirin independent of changes in blood pressure. Salt loading significantly increased superoxide production in basilar arteries of SHRSP, which were significantly suppressed by treatment with aspirin. Salt loading also significantly decreased NOS activity in the basilar arteries of SHRSP, which were significantly improved by treatment with aspirin. At 5 weeks after salt loading, macrophage accumulation and matrix metalloproteinase-9 activity at the stroke-negative area in cerebral cortex of SHRSP were significantly reduced by treatment with aspirin. These results suggest that low-dose aspirin may exert protective effects against cerebrovascular inflammation and damage by salt loading through down-regulation of superoxide production and induction of nitric oxide synthesis.

  7. Acetylsalicylic acid (ASA) - How much, how often, and when? A clinical-pharmacological perspective.

    Science.gov (United States)

    Loew, Dieter; Belz, Gustav G

    2016-08-01

    The dose of acetylsalicylic acid (ASA) commonly used in the prevention and treatment of arteriosclerotic angiopathies is equal to or less than 100 mg daily. This choice of dose is predominantly based on molecular-pharmacological findings showing an inhibition in synthesis of the prothrombotic thromboxane (TXB2) and an irreversible inhibition in blood platelet aggregation. However, an analysis of ASA dose-effect relationships for doses of 50 - 500 mg (PO and IV) shows that doses of ASA up to 100 mg daily produce only a small or moderate inhibition in collagen/epinephrine-induced platelet aggregation and have no significant effect on the important platelet factors, PF3 and PF4. Doses of ASA 300 - 500 mg, on the other hand, inhibit platelet aggregation almost completely and, in addition, produce a 50 - 70% inhibition in PF3 and PF4 lasting at least 24 hours. There is also evidence that doses of ASA above 100 mg daily markedly inhibit thromboxane synthesis for up to 24 hours and that doses of 500 mg daily produce a clinically relevant inhibition in platelet adhesion to vessel walls for up 72 hours and prevent procoagulatory shape changes for up to 12 hours. These findings suggest that a dose of ≥ 300 mg at intervals of 2 - 3 days would be more appropriate for primary and secondary prophylaxis of arteriosclerotic angiopathies and that the benefit-risk ratio would be greater because of the increased availability of mucoprotective prostaglandins, PGI2 (prostacyclin) and the gastroprotective, PGE2. Our viewpoint, predominantly based on findings with biomarkers, could serve as a basis for further randomized controlled studies.

  8. Local sustained delivery of acetylsalicylic acid via hybrid stent with biodegradable nanofibers reduces adhesion of blood cells and promotes reendothelialization of the denuded artery

    Directory of Open Access Journals (Sweden)

    Lee CH

    2014-01-01

    Full Text Available Cheng-Hung Lee,1,2 Yu-Huang Lin,3 Shang-Hung Chang,1 Chun-Der Tai,3 Shih-Jung Liu,2 Yen Chu,4 Chao-Jan Wang,5 Ming-Yi Hsu,5 Hung Chang,6 Gwo-Jyh Chang,7 Kuo-Chun Hung,1 Ming-Jer Hsieh,1 Fen-Chiung Lin,1 I-Chang Hsieh,1 Ming-Shien Wen,1 Yenlin Huang81Division of Cardiology, Department of Internal Medicine, Chang Gung Memorial Hospital, Chang Gung University College of Medicine, Linkou, 2Department of Mechanical Engineering, 3Graduate Institute of Medical Mechatronics, Chang Gung University, 4Laboratory of Cardiovascular Physiology, Division of Thoracic and Cardiovascular Surgery, 5Department of Medical Imaging and Intervention, 6Hematology-Oncology Division, Department of Internal Medicine, Chang Gung Memorial Hospital, Linkou, 7Graduate Institute of Clinical Medicinal Sciences, Chang Gung University College of Medicine, Linkou, 8Department of Anatomical Pathology, Chang Gung Memorial Hospital, Linkou, Tao-Yuan, TaiwanAbstract: Incomplete endothelialization, blood cell adhesion to vascular stents, and inflammation of arteries can result in acute stent thromboses. The systemic administration of acetylsalicylic acid decreases endothelial dysfunction, potentially reducing thrombus, enhancing vasodilatation, and inhibiting the progression of atherosclerosis; but, this is weakened by upper gastrointestinal bleeding. This study proposes a hybrid stent with biodegradable nanofibers, for the local, sustained delivery of acetylsalicylic acid to injured artery walls. Biodegradable nanofibers are prepared by first dissolving poly(D,L-lactide-co-glycolide and acetylsalicylic acid in 1,1,1,3,3,3-hexafluoro-2-propanol. The solution is then electrospun into nanofibrous tubes, which are then mounted onto commercially available bare-metal stents. In vitro release rates of pharmaceuticals from nanofibers are characterized using an elution method, and a high-performance liquid chromatography assay. The experimental results suggest that biodegradable nanofibers

  9. Acetylsalicylic acid interferes with embryonic kidney growth and development by a prostaglandin-independent mechanism

    Science.gov (United States)

    Welham, Simon J M; Sparrow, Alexander J; Gardner, David S; Elmes, Matthew J

    2017-01-01

    AIM To evaluate the effects of the non-selective, non-steroidal anti-inflammatory drug (NSAID) acetylsalicylic acid (ASA), on ex vivo embryonic kidney growth and development. METHODS Pairs of fetal mouse kidneys at embryonic day 12.5 were cultured ex vivo in increasing concentrations of ASA (0.04-0.4 mg/mL) for up to 7 d. One organ from each pair was grown in control media and was used as the internal control for the experimental contralateral organ. In some experiments, organs were treated with ASA for 48 h and then transferred either to control media alone or control media containing 10 μmol/L prostaglandin E2 (PGE2) for a further 5 d. Fetal kidneys were additionally obtained from prostaglandin synthase 2 homozygous null or heterozygous (PTGS2-/- and PTGS2-/+) embryos and grown in culture. Kidney cross-sectional area was used to determine treatment effects on kidney growth. Whole-mount labelling to fluorescently detect laminin enabled crude determination of epithelial branching using confocal microscopy. RESULTS Increasing ASA concentration (0.1, 0.2 and 0.4 mg/mL) significantly inhibited metanephric growth (P < 0.05). After 7 d of culture, exposure to 0.2 mg/mL and 0.4 mg/mL reduced organ size to 53% and 23% of control organ size respectively (P < 0.01). Addition of 10 μmol/L PGE2 to culture media after exposure to 0.2 mg/mL ASA for 48 h resulted in a return of growth area to control levels. Application of control media alone after cessation of ASA exposure showed no benefit on kidney growth. Despite the apparent recovery of growth area with 10 μmol/L PGE2, no obvious renal tubular structures were formed. The number of epithelial tips generated after 48 h exposure to ASA was reduced by 40% (0.2 mg/mL; P < 0.05) and 47% (0.4 mg/mL; P < 0.01). Finally, growth of PTGS2-/- and PTGS2+/- kidneys in organ culture showed no differences, indicating that PTGS2 derived PGE2 may at best have a minor role. CONCLUSION ASA reduces early renal growth and development but the

  10. Novel {beta}-cyclodextrin modified CdTe quantum dots as fluorescence nanosensor for acetylsalicylic acid and metabolites

    Energy Technology Data Exchange (ETDEWEB)

    Algarra, M. [Centro de Geologia do Porto, Faculdade de Ciencias, Universidade do Porto, Rua do Campo Alegre 687, 4169-007 Porto (Portugal); Campos, B.B.; Aguiar, F.R.; Rodriguez-Borges, J.E. [Centro de Investigacao em Quimica (CIQ-UP), Faculdade de Ciencias da Universidade do Porto, Rua do Campo Alegre 687, 169-007 Porto (Portugal); Esteves da Silva, J.C.G., E-mail: jcsilva@fc.up.pt [Centro de Investigacao em Quimica (CIQ-UP), Faculdade de Ciencias da Universidade do Porto, Rua do Campo Alegre 687, 169-007 Porto (Portugal)

    2012-05-01

    {beta}-Cyclodextrin was modified with 11-[(ethoxycarbonyl)thio]undecanoic acid and used as a capping agent, together with mercaptosuccinic acid, to prepare water-stable CdTe quantum dots. The water soluble quantum dot obtained displays fluorescence with a maximum emission at 425 nm (under excitation at 300 nm) with lifetimes of 0.53, 4.8, 181, and 44.1 ns, respectively. The S-{beta}CD-MSA-CdTe can act as a nanoprobe that is due to the affinity of the cyclodextrin moiety for selected substances such as acetylsalicylic acid (ASA) and its metabolites as foreign species. The fluorescence of the S-{beta}CD-MSA-CdTe is enhanced on addition of ASA. Linear calibration plots are observed with ASA in concentrations between 0 and 1 mg/l, with a limit of detection at 8.5 Multiplication-Sign 10{sup -9} mol/l (1.5 ng/ml) and a precision as relative standard deviation of 1% (0.05 mg/l). The interference effect of certain compounds as ascorbic acid and its main metabolites such as salicylic, gentisic and salicyluric acid upon the obtained procedure was studied. Highlights: Black-Right-Pointing-Pointer Nanosensors constituted by CdTe quantum dots capped with modified cyclodextrin. Black-Right-Pointing-Pointer This nanomaterial shows fluorescence properties compatible with a semiconductor quantum dot. Black-Right-Pointing-Pointer The nanosensor shows fluorescence enhancement when inclusion complexes are formed with acetylsalicylic acid. Black-Right-Pointing-Pointer This nanomaterial has nanosensor potential taking into consideration the formation stability of the inclusion complex.

  11. Impact of low-dose acetylsalicylic acid on kidney function in type 2 diabetic patients with elevated urinary albumin excretion rate

    DEFF Research Database (Denmark)

    Gaede, Peter; Hansen, Henrik Post; Parving, Hans-Henrik

    2003-01-01

    Low-dose treatment with acetylsalicylic acid (ASA) is widely recommended to type 2 diabetic patients as primary prevention against cardiovascular disease. High-dose treatment with cyclooxygenase inhibitors reduces urinary albumin excretion rate (AER) in type 1 diabetic patients with micro...

  12. The effect of low-dose acetylsalicylic acid on bleeding after transurethral prostatectomy--a prospective, randomized, double-blind, placebo-controlled study

    DEFF Research Database (Denmark)

    Nielsen, Jesper Dan; Holm-Nielsen, A; Jespersen, J

    2000-01-01

    OBJECTIVE: An increase in the loss of blood after ingestion of acetylsalicylic acid (ASA) has been reported after several types of surgery, but randomized placebo-controlled studies have exclusively been performed after coronary artery bypass surgery. The reported effects of ASA on bleeding after...

  13. The Effect of Roux-en-Y Gastric Bypass Surgery in Morbidly Obese Patients on Pharmacokinetics of (Acetyl)Salicylic Acid and Omeprazole : the ERY-PAO Study

    NARCIS (Netherlands)

    Mitrov-Winkelmolen, Lieke; van Buul-Gast, Marie-Christine W.; Swank, Dingeman J.; Overdiek, Hans W. P. M.; van Schaik, Ron H. N.; Touw, Daan J.

    2016-01-01

    Data on the absorption of orally administered drugs following Roux-en-Y gastric bypass (RYGB) surgery in obese patients are limited and inconclusive. As it is difficult to predict changes in absorption, studies on frequently used drugs in this population are necessary. Acetylsalicylic acid (ASA) and

  14. Continuation of medically necessary platelet aggregation inhibitors - acetylsalicylic acid and clopidogrel - during surgery for spinal degenerative disorders: Results in 100 patients

    Directory of Open Access Journals (Sweden)

    Reza Akhavan-Sigari

    2014-01-01

    Full Text Available Background: Patients undergoing spinal surgery while under anticoagulation therapy are at risk of developing bleeding complications, even though lower incidences have been reported for joint arthroplasty surgery. There is a gap in the medical literature examining the incidence of postoperative spinal bleeding in patients who were under anticoagulation medication at the time of surgery. Methods: We prospectively followed a consecutive cohort of 100 patients (58 male, 42 female undergoing spinal surgery. The average patient age was 48.7 years and the minimum follow up time was 12 months. Diagnosis was lumbar spinal stenosis in 20, herniated lumbar discs in 63, degenerative cervical disc disease in 3, and cervical disc herniation in 14 cases. In our study, platelet aggregation inhibitors (clopidogrel and/or acetylsalicylic acid were given for the treatment of cardiovascular and cerebrovascular thrombotic events, to reduce risk of stroke in patients who have had transient ischemia of the brain or acute coronary syndrome, and as secondary prevention of atherosclerotic events (fatal or nonfatal myocardial infarction (MI. A cessation of anticoagulants (acetylsalicylic acid or clopidogrel in our patients in the peri- and postoperative period was contraindicated. Results: Sixty-three patients were on both clopidogrel and acetylsalicylic acid and 37 on acetylsalicylic acid only. None of the patients suffered any postoperative bleeding complication. Three patients suffered postoperative wound dehiscence and one patient had an infection that required reoperation. Conclusion: The question of whether preoperative platelet aggregation inhibitors must be stopped before elective spinal surgery has never been answered in the literature. In our prospective series, we have found no increase in the risk of postoperative spinal bleeding with the use of clopidogrel or acetylsalicylic acid. This finding suggests that spine surgery can be done without stopping

  15. Induction of omega-oxidation of monocarboxylic acids in rats by acetylsalicylic acid.

    Science.gov (United States)

    Kundu, R K; Tonsgard, J H; Getz, G S

    1991-12-01

    The accumulation of dicarboxylic acids, particularly long chain, is a prominent feature of Reye's syndrome and diseases of peroxisomal metabolism. We assessed the omega-oxidation of a spectrum of fatty acids in rats and asked whether pretreatment of rats with aspirin, which is known to predispose children to Reye's syndrome, would affect omega-oxidation of long chain fatty acids. We found that aspirin increased liver free fatty acids and increased the capacity for omega-oxidation three- to sevenfold. Omega-oxidation of long chain substrate was stimulated to a greater degree than medium chain substrate and was apparent within one day of treatment, at serum aspirin concentrations below the therapeutic range in humans. The apparent Km for lauric acid was 0.9 microM and 12 microM for palmitate. We also found a difference in the storage stability of activity toward medium and long chain substrate. Saturating concentrations of palmitate had no effect on the formation of dodecanedioic acid, whereas laurate decreased but never eliminated the omega-oxidation of palmitate. 97% of the total laurate omega-oxidative activity recovered was found in the microsomes, but 32% of palmitate omega-oxidative activity was present in the cytosol. These results demonstrate that aspirin is a potent stimulator of omega-oxidation and suggest that there may be multiple enzymes for omega-oxidation with overlapping substrate specificity.

  16. The study on the interaction between Tb(III) and ligand in Tb-acetylsalicylic acid complex and fluorescence mechanism

    Energy Technology Data Exchange (ETDEWEB)

    Wu Wenru; Rong Yuzhi; Zhao Bo [Jiangsu Key Laboratory of Biofunctional Materials, College of Chemistry and Environmental Science, Nanjing Normal University, Nanjing, 210097 (China); Sun Peipei, E-mail: sunpeipei@njnu.edu.c [Jiangsu Key Laboratory of Biofunctional Materials, College of Chemistry and Environmental Science, Nanjing Normal University, Nanjing, 210097 (China); Huang Xiaohua, E-mail: huangxiaohua@njnu.edu.c [Jiangsu Key Laboratory of Biofunctional Materials, College of Chemistry and Environmental Science, Nanjing Normal University, Nanjing, 210097 (China)

    2010-01-15

    In this paper, a luminescent complex of terbium-acetylsalicylic acid (Tb-ASA) was studied for the first time using combination of the quantum chemical calculation, fluorescence spectroscopic method and X-ray photoelectron spectroscopy (XPS). The results from the quantum chemical calculation indicated that it is possible for the energy-transfer from ASA to Tb (III); Fluorescence spectroscopy demonstrated that there is an intramolecular energy-transfer from ASA to Tb with the efficiency (III) of about 87.9% under an excitation at 308 nm. The XPS indicated that the coordinate covalent bond between Tb and O existed in the complex of Tb-ASA leads to the effective energy transfer from ASA to Tb (III) because the energy transfer rate may be improved with reducing the distance between the ligand and Tb (III). The results will have important values for the studies of this type of complexes.

  17. Simultaneous determination of acetylsalicylic acid and salicylic acid in human plasma by isocratic high-pressure liquid chromatography with post-column hydrolysis and fluorescence detection.

    Science.gov (United States)

    Hobl, Eva-Luise; Jilma, Bernd; Ebner, Josef; Schmid, Rainer W

    2013-06-01

    A selective, sensitive and rapid high-performance liquid chromatography method with post-column hydrolysis and fluorescence detection was developed for the simultaneous quantification of acetylsalicylic acid and its metabolite salicylic acid in human plasma. Following the addition of 2-hydroxy-3-methoxybenzoic acid as internal standard and simple protein precipitation with acetonitrile, the analytes were separated on a ProntoSIL 120 C18 ace-EPS column (150 × 2 mm, 3 µm) protected by a C8 guard column (5 µm). The mobile phase, 10 mm formic acid in water (pH 2.9) and acetonitrile (70:30, v/v), was used at a flow rate of 0.35 mL/min. After on-line post-column hydrolysis of acetylsalicylic acid (ASA) to salicylic acid (SA) by addition of alkaline solution, the analytes were measured at 290 nm (λex ) and 400 nm (λem ). The method was linear in the concentration ranges between 0.05 and 20 ng/μL for both ASA and SA with a lower limit of quantification of 25 pg/μL for SA and 50 pg/μL for ASA. The limit of detection was 15 pg/μL for SA and 32.5 pg/μL for ASA. The analysis of ASA and SA can be carried out within 8 min; therefore this method is suitable for measuring plasma concentrations of salicylates in clinical routine.

  18. Formation of molecular complexes of salicylic acid, acetylsalicylic acid, and methyl salicylate in a mixture of supercritical carbon dioxide with a polar cosolvent

    Science.gov (United States)

    Petrenko, V. E.; Antipova, M. L.; Gurina, D. L.; Odintsova, E. G.

    2015-08-01

    The solvate structures formed by salicylic acid, acetylsalicylic acid, and methyl salicylate in supercritical (SC) carbon dioxide with a polar cosolvent (methanol, 0.03 mole fractions) at a density of 0.7 g/cm3 and a temperature of 318 K were studied by the molecular dynamics method. Salicylic and acetylsalicylic acids were found to form highly stable hydrogen-bonded complexes with methanol via the hydrogen atom of the carboxyl group. For methyl salicylate in which the carboxyl hydrogen is substituted by a methyl radical, the formation of stable hydrogen bonds with methanol was not revealed. The contribution of other functional groups of the solute to the interactions with the cosolvent was much smaller. An analysis of correlations between the obtained data and the literature data on the cosolvent effect on the solubility of the compounds in SC CO2 showed that the dissolving ability of SC CO2 with respect to a polar organic substance in the presence of a cosolvent increased only when stable hydrogen-bonded complexes are formed between this substance and the cosolvent.

  19. COST-EFFECTIVENESS OF APIXABAN AS COMPARED WITH WARFARIN AND ACETYLSALICYLIC ACID IN PATIENTS WITH NON-VALVULAR ATRIAL FIBRILLATION IN THE RUSSIAN FEDERATION

    Directory of Open Access Journals (Sweden)

    A. V. Rudakova

    2015-09-01

    Full Text Available Background. For prevention of thromboembolic events in patients with non-valvular atrial fibrillation (NVAF the following types of antithrombotic therapy are used: anticoagulant therapy with vitamin K antagonists (such as warfarin, antiplatelet therapy (such as acetylsalicylic acid and novel oral anticoagulants such as apixaban, rivaroxaban and dabigatran. Administration of vitamin K antagonists (VKA is complicated by the need for individual dose adjustment and frequent monitoring of international normalized ratio (INR. Both warfarin and acetylsalicylic acid are widely used for thrombosis prevention in patients with NVAF in the Russian Federation.Aim. To evaluate the cost-effectiveness ratio of apixaban compared with warfarin and acetylsalicylic acid in patients with NVAF from the Russian Federation national health care system perspective.Material and methods. This analysis used a Markov model that allowed estimation of the incremental cost-effectiveness ratio (ICER for apixaban as compared with warfarin and acetylsalicylic acid over lifetime horizon in VKA suitable and VKA unsuitable patients with NVAF respectively. The model enclosed cardiovascular event rates based on the results of the randomized clinical trials comparing clinical effectiveness and safety of apixaban with warfarin (ARISTOTLE and acetylsalicylic acid (AVERROES. The following cardiovascular events were taken into consideration: ischemic and hemorrhagic stroke, systemic embolism, intracranial hemorrhage, other major bleeds, clinically relevant non-major bleeds and myocardial infarction. Direct medical costs were determined based on the rates of the compulsory national medical insurance system. The price of the antithrombotic drugs was taken as a weighted average tender price for the year 2013. In the model both costs and benefits (quality-adjusted life years and life-years were discounted at 3.5%. Cost-effectiveness threshold was set at 1.4 million rubles per quality

  20. COST-EFFECTIVENESS OF APIXABAN AS COMPARED WITH WARFARIN AND ACETYLSALICYLIC ACID IN PATIENTS WITH NON-VALVULAR ATRIAL FIBRILLATION IN THE RUSSIAN FEDERATION

    Directory of Open Access Journals (Sweden)

    A. V. Rudakova

    2014-01-01

    Full Text Available Background. For prevention of thromboembolic events in patients with non-valvular atrial fibrillation (NVAF the following types of antithrombotic therapy are used: anticoagulant therapy with vitamin K antagonists (such as warfarin, antiplatelet therapy (such as acetylsalicylic acid and novel oral anticoagulants such as apixaban, rivaroxaban and dabigatran. Administration of vitamin K antagonists (VKA is complicated by the need for individual dose adjustment and frequent monitoring of international normalized ratio (INR. Both warfarin and acetylsalicylic acid are widely used for thrombosis prevention in patients with NVAF in the Russian Federation.Aim. To evaluate the cost-effectiveness ratio of apixaban compared with warfarin and acetylsalicylic acid in patients with NVAF from the Russian Federation national health care system perspective.Material and methods. This analysis used a Markov model that allowed estimation of the incremental cost-effectiveness ratio (ICER for apixaban as compared with warfarin and acetylsalicylic acid over lifetime horizon in VKA suitable and VKA unsuitable patients with NVAF respectively. The model enclosed cardiovascular event rates based on the results of the randomized clinical trials comparing clinical effectiveness and safety of apixaban with warfarin (ARISTOTLE and acetylsalicylic acid (AVERROES. The following cardiovascular events were taken into consideration: ischemic and hemorrhagic stroke, systemic embolism, intracranial hemorrhage, other major bleeds, clinically relevant non-major bleeds and myocardial infarction. Direct medical costs were determined based on the rates of the compulsory national medical insurance system. The price of the antithrombotic drugs was taken as a weighted average tender price for the year 2013. In the model both costs and benefits (quality-adjusted life years and life-years were discounted at 3.5%. Cost-effectiveness threshold was set at 1.4 million rubles per quality

  1. Preharvest treatments with malic, oxalic, and acetylsalicylic acids affect the phenolic composition and antioxidant capacity of coriander, dill and parsley.

    Science.gov (United States)

    El-Zaeddi, Hussein; Calín-Sánchez, Ángel; Nowicka, Paulina; Martínez-Tomé, Juan; Noguera-Artiaga, Luis; Burló, Francisco; Wojdyło, Aneta; Carbonell-Barrachina, Ángel A

    2017-07-01

    The effects of a preharvest treatment with malic (MA), oxalic (OA), or acetylsalicylic (ASA) acid at three concentrations (1, 2 and 3mM) on the bioactivity and antioxidant capacity of coriander, dill, and parsley were investigated. The antioxidant capacity of the herbs extracts was assayed by spectrophotometric methods by using three different analytical methods: ORAC, FRAP, and ABTS; the effects of treatments were very positive in coriander, produced intermediate results in dill, and no effects were found in parsley plants. Polyphenol compounds were identified by LC-MS-QTof and quantified by UPLC-PDA-FL. Thirty phenolic compounds were identified in these three herbs. The major compounds were (i) coriander: dimethoxycinnamoyl hexoside and quercetin-3-O-rutinoside, (ii) dill: neochlorogenic acid and quercetin glucuronide, and (iii) parsley: apigenin-7-apiosylglucoside (apiin) and isorhamnetin-3-O-hexoside. The application of these three organic acids favored the accumulation of phenolic compounds in coriander plants, but had no significant positive effects on dill and parsley. The treatments leading to the best results in all three plants were the application of MA or OA at 1mM.

  2. Simultaneous quantitation of acetylsalicylic acid and clopidogrel along with their metabolites in human plasma using liquid chromatography tandem mass spectrometry.

    Science.gov (United States)

    Chhonker, Yashpal S; Pandey, Chandra P; Chandasana, Hardik; Laxman, Tulsankar Sachin; Prasad, Yarra Durga; Narain, V S; Dikshit, Madhu; Bhatta, Rabi S

    2016-03-01

    The interest in therapeutic drug monitoring has increased over the last few years. Inter- and intra-patient variability in pharmacokinetics, plasma concentration related toxicity and success of therapy have stressed the need of frequent therapeutic drug monitoring of the drugs. A sensitive, selective and rapid liquid chromatography coupled with tandem mass spectrometry (LC-MS/MS) method was developed for the simultaneous quantification of acetylsalicylic acid (aspirin), salicylic acid, clopidogrel and carboxylic acid metabolite of clopidogrel in human plasma. The chromatographic separations were achieved on Waters Symmetry Shield(TM) C18 column (150 × 4.6 mm, 5 µm) using 3.5 mm ammonium acetate (pH 3.5)-acetonitrile (10:90, v/v) as mobile phase at a flow rate of 0.75 mL/min. The present method was successfully applied for therapeutic drug monitoring of aspirin and clopidogrel in 67 patients with coronary artery disease.

  3. Binding modes of aromatic ligands to mammalian heme peroxidases with associated functional implications: crystal structures of lactoperoxidase complexes with acetylsalicylic acid, salicylhydroxamic acid, and benzylhydroxamic acid.

    Science.gov (United States)

    Singh, Amit K; Singh, Nagendra; Sinha, Mau; Bhushan, Asha; Kaur, Punit; Srinivasan, Alagiri; Sharma, Sujata; Singh, Tej P

    2009-07-24

    The binding and structural studies of bovine lactoperoxidase with three aromatic ligands, acetylsalicylic acid (ASA), salicylhydoxamic acid (SHA), and benzylhydroxamic acid (BHA) show that all the three compounds bind to lactoperoxidase at the substrate binding site on the distal heme side. The binding of ASA occurs without perturbing the position of conserved heme water molecule W-1, whereas both SHA and BHA displace it by the hydroxyl group of their hydroxamic acid moieties. The acetyl group carbonyl oxygen atom of ASA forms a hydrogen bond with W-1, which in turn makes three other hydrogen-bonds, one each with heme iron, His-109 N(epsilon2), and Gln-105 N(epsilon2). In contrast, in the complexes of SHA and BHA, the OH group of hydroxamic acid moiety in both complexes interacts with heme iron directly with Fe-OH distances of 3.0 and 3.2A respectively. The OH is also hydrogen bonded to His-109 N(epsilon2) and Gln-105N(epsilon2). The plane of benzene ring of ASA is inclined at 70.7 degrees from the plane of heme moiety, whereas the aromatic planes of SHA and BHA are nearly parallel to the heme plane with inclinations of 15.7 and 6.2 degrees , respectively. The mode of ASA binding provides the information about the mechanism of action of aromatic substrates, whereas the binding characteristics of SHA and BHA indicate the mode of inhibitor binding.

  4. COMPARISON OF ANTIPLATELET EFFICACY OF ORIGINAL AND GENERIC ENTEROSOLUBLE ACETYLSALICYLIC ACID IN PATIENTS WITH HIGH CARDIOVASCULAR RISK. SIMPLE BLIND CROSSED RANDOMIZED CONTROLLED STUDY (IKAR)

    OpenAIRE

    2010-01-01

    Aim. To compare the antiplatelet efficacy of the original and generic enterosoluble tableted acetylsalicylic acid (ASA) in patients with high cardiovascular risk.Material and мethods. Patients (n=30) with high cardiovascular risk and indications for the ASA therapy were included in the study. Antiplatelet agents were withdrawn 3 weeks before study start (wash-out period). Study drugs were distributed at the start visit according to the randomization scheme. The first study drug course was 3 w...

  5. Acetylsalicylic acid-induced changes in the chemical coding of extrinsic sensory neurons supplying the prepyloric area of the porcine stomach.

    Science.gov (United States)

    Rytel, L; Calka, J

    2016-03-23

    Acetylsalicylic acid is a popular drug that is commonly used to treat fever and inflammation, but which can also negativity affect the mucosal layer of the stomach, although knowledge concerning its influence on gastric innervation is very scarce. Thus, the aim of the present study was to study the influence of prolonged acetylsalicylic acid supplementation on the extrinsic primary sensory neurons supplying the porcine stomach prepyloric region. Fast Blue (FB) was injected into the above-mentioned region of the stomach. Acetylsalicylic acid was then given orally to the experimental gilts from the seventh day after FB injection to the 27th day of the experiment. After euthanasia, the nodose ganglia (NG) and dorsal root ganglia (DRG) were collected. Sections of these ganglia were processed for routine double-labelling immunofluorescence technique for substance P (SP), calcitonine gene related peptide (CGRP), galanin (GAL), neuronal isoform of nitric oxide synthase (nNOS) and vasoactive intestinal polypeptide (VIP). Under physiological conditions within the nodose ganglia, the percentage of the FB-labeled neurons immunoreactive to particular substances ranged between 17.9 ± 2.7% (VIP-like immunoreactive (LI) neurons in the right NG) and 60.4 ± 1.7% (SP-LI cells within the left NG). Acetylsalicylic acid supplementation caused a considerable increase in the expression of all active substances studied within both left and right NG and the percentage of neurons positive to particular substances fluctuated from 47.2 ± 3.6% (GAL-LI neurons in the right NG) to 67.2 ± 2.0% (cells immunoreactive to SP in the left NG). All studied substances were also observed in DRG neurons supplying the prepyloric region of the stomach, but the number of immunoreactive neurons was too small to conduct a statistical analysis. The obtained results show that ASA may influence chemical coding of the sensory neurons supplying the porcine stomach, but the exact mechanisms of this action still

  6. Salicylate antagonism of acetylsalicylic acid inhibition of platelet aggregation in male and female subjects: influence of citrate concentration.

    Science.gov (United States)

    Philp, R B; Paul, M L

    1986-01-01

    Platelets from volunteers were exposed for 1 min to sodium salicylate (SA) before and after the addition of acetylsalicylic acid (ASA) to produce greater than or equal to 50% inhibition of aggregation induced by arachidonic acid (AA) or collagen. SA:ASA concentrations = 20:1. SA protection against ASA inhibition was always observed even if ASA exposure time was 15 min, whereas reversal could not be demonstrated once exposure of platelets to ASA exceeded a minimum of 3-10 min with AA as the stimulus. Reversal was even less effective when collagen was the stimulus. An apparent, increased sensitivity to SA reversal of ASA inhibition in females disappeared when citrate concentration was adjusted to compensate for lower packed cell volume. The proposed male dependency for protection in ASA treatment of thromboembolic disorders cannot be explained on the basis of differences in the SA-ASA competition at platelet cyclooxygenase and, if collagen is an important in vivo stimulus of platelet interaction with damaged vessel wall, the antagonism of ASA by SA may not be important.

  7. A Prevention of Pre-eclampsia with the Use of Acetylsalicylic Acid and Low-molecular Weight Heparin - Molecular Mechanisms.

    Science.gov (United States)

    Darmochwal-Kolarz, Dorota; Kolarz, Bogdan; Korzeniewski, Michal; Kimber-Trojnar, Zaneta; Patro-Malysza, Jolanta; Mierzynski, Radzisław; Przegalinska-Kałamucka, Monika; Oleszczuk, Jan

    Pre-eclampsia appears to be the main cause for the maternal and fetal morbidity and mortality. Pregnant women with pre-eclampsia are more likely to be threatened with conditions which potentially may be lethal, such as: disseminated intravascular coagulation, cerebral hemorrhage, liver and renal failure. Pregnancy complicated with pre-eclampsia is also associated with a greater risk for iatrogenic prematurity, intrauterine growth retardation, premature abruption of placenta, and even intrauterine fetal death. In the majority of cases the reasons for arterial hypertension among pregnant women remain obscure. For the past decades, there were many abortive attempts in the use of some microelements, vitamins or specific diets, such as polyunsaturated fatty acids, for the prophylaxis of pre-eclampsia. Recently, it has been shown that a prevention of pre-eclampsia with the use of a lowmolecular- weight heparins (LMWHs) and acetylsalicylic acid (ASA) could considerably reduce the frequency of preeclampsia. In this review, we present the studies concerning the applications of LMWHs and aspirin in the prophylaxis of pre-eclampsia and some important data about the mechanisms of anti-inflammatory actions of LMWHs and ASA.

  8. On the origin of surface imposed anisotropic growth of salicylic and acetylsalicylic acids crystals during droplet evaporation.

    Science.gov (United States)

    Przybyłek, Maciej; Cysewski, Piotr; Pawelec, Maciej; Ziółkowska, Dorota; Kobierski, Mirosław

    2015-03-01

    In this paper droplet evaporative crystallization of salicylic acid (SA) and acetylsalicylic acid (ASA) crystals on different surfaces, such as glass, polyvinyl alcohol (PVA), and paraffin was studied. The obtained crystals were analyzed using powder X-ray diffraction (PXRD) technique. In order to better understand the effect of the surface on evaporative crystallization, crystals deposited on glass were scraped off. Moreover, evaporative crystallization of a large volume of solution was performed. As we found, paraffin which is non-polar surface promotes formation of crystals morphologically similar to those obtained via bulk evaporative crystallization. On the other hand, when crystallization is carried out on the polar surfaces (glass and PVA), there is a significant orientation effect. This phenomenon is manifested by the reduction of the number of peaks in PXRD spectrum recorded for deposited on the surface crystals. Noteworthy, reduction of PXRD signals is not observed for powder samples obtained after scraping crystals off the glass. In order to explain the mechanism of carboxylic crystals growth on the polar surfaces, quantum-chemical computations were performed. It has been found that crystal faces of the strongest orientation effect can be characterized by the highest surface densities of intermolecular interactions energy (IIE). In case of SA and ASA crystals formed on the polar surfaces the most dominant faces are characterized by the highest adhesive and cohesive properties. This suggests that the selection rules of the orientation effect comes directly from surface IIE densities.

  9. Hydrogen atoms in acetylsalicylic acid (Aspirin): the librating methyl group and probing the potential well in the hydrogen-bonded dimer

    Science.gov (United States)

    Wilson, Chick C.

    2001-02-01

    The structure of acetylsalicylic acid (2-(acetoyloxy)benzoic acid; Aspirin) has been studied by variable temperature single crystal neutron diffraction. The usual large torsional librational motion of the terminal methyl group is observed and its temperature dependence analysed using a simple model for the potential, yielding the force constant and barrier height for this motion. In addition, asymmetry of the scattering density of the proton involved in the hydrogen bond forming the carboxylic acid dimer motif is observed at temperatures above 200 K. This asymmetry is discussed in terms of its possible implications for the shape of the hydrogen bonding potential well.

  10. Effect of roxatidine bismuth citrate (MX1) against acetylsalicylic acid- and indomethacin-induced gastric mucosal damage in rats.

    Science.gov (United States)

    Marazova, K; Klouchek, E; Popov, A; Ivanov, C; Krushkov, I; Ichikawa, T; Ishihara, K; Hotta, K

    1998-10-01

    We have studied the effect of the newly synthesized agent, roxatidine bismuth citrate (N-[3-(3-(1-piperidinyl-methyl)phenoxy)propyl]-hydroxyacetamide-2- hydroxypropane-1,2,3-tricarboxylate-bismuth(3+) complex), code name MX1, against acetylsalicylic acid (ASA)- and indomethacin-induced gastric mucosal damage in rats. Effects of MX1 (12.5, 50, 125, 184, 250 mg/kg) were compared to the effects of equimolar doses of roxatidine and bismuth subcitrate. Effect of MX1 (10(-6) M) on mucin biosynthesis measured by [3H] glucosamine incorporation in rat gastric corpus has been determined. MX1-pretreatment dose-dependently decreased the mean ulcer number and length in all doses used in an extent similar to that of roxatidine and more pronounced in comparison with bismuth subcitrate. The morphometrical results have been confirmed histomorphologically. The biosynthesis of mucin was found to be significantly enhanced after MX1 addition. The results of the present study suggest that MX1 has a gastroprotective effect against ASA- and indomethacin-induced ulcers which might be due both to its H2-blocking and mucus-stimulating activity.

  11. Characterization of a dextran–coated layered double hydroxide acetylsalicylic acid delivery system and its pharmacokinetics in rabbit

    Directory of Open Access Journals (Sweden)

    Li-e Dong

    2013-12-01

    Full Text Available The aim of this study was to prepare a dextran–coated layered double hydroxide acetylsalicylic acid (DEX–LDH–ASA delivery system by co-precipitation of LDH–ASA and its in-situ compositing with DEX. The structure of the system was investigated using X-ray diffraction (XRD, Fourier transform infrared spectroscopy (FT-IR and thermogravimetry (TG. Its in vitro drug release properties and in vivo pharmacokinetics in rabbit were also determined. The results show that the DEX–LDH–ASA system retained the crystal structure of LDH–ASA and gave a marked improvement in its dispersion. It also prolonged the release of ASA and shifted the release pattern from first-order to zero-order kinetics. The pharmacokinetics of ASA administered in the DEX–LDH–ASA system to rabbits produced two absorption peaks with a Cmax of 14.8±1.7 mg/L at 2.11±0.69 h and an elimination half-life of 2.25±0.84 h for the first peak. The fact that delivery of ASA in the DEX–LDH–ASA system was sustained with improved bioavailability indicates the potential of the system as a controlled release formulation with application to other drugs.

  12. RISK OF REPEATED THROMBOTIC EVENTS IN PATIENTS SURVIVED ACUTE CORONARY SYNDROME AND HAVING LABORATORY PROVEN RESISTANCE TO ACETYLSALICYLIC ACID

    Directory of Open Access Journals (Sweden)

    N. F. Puchinyan

    2009-01-01

    Full Text Available Aim. To evaluate risk of repeated atherothrombotic events in patients survived acute coronary syndrome (ACS and having poorly reduced platelet aggregation (proven by optical aggregometry in response to acetylsalicylic acid (ASA therapy.Material and methods. 200 patients with ACS (aged 56,6±9,2 y.o. were included in the study. Platelet functional activity during ASA therapy was evaluated with laser aggregometer. ASA resistance was defined if the summarizing index of platelet aggregation (induced with ADP, 5 mμml/l was 50% or higher during ASA therapy. Observation period was 18±6 months. Atherothrombotic events (unstable angina, myocardial infarction, stroke, cardiovascular death were considered.Results. Lack ASA response rate was about 12%. Totally 22 repeated atherothrombotic events were registered: 5,6% among ASA sensitive patients and 50% - among ASA resistant patients. Repeated atherothrombotic events were registered in ASA resistance patients during first 14 days. ASA sensitive patients showed repeated atherothrombotic events in some months after ACS. The relative risk of cardiovascular event in ASA resistance patients was 8,92 (CI 95% 4,39; 17,84 р=0,05.Conclusion. The high level of the induced platelet aggregation (proven by laser aggregometry points to high risk of repeated atherothrombotic events in patients with ACS.

  13. Inhibition of Radiation-Induced Oxidative Damage in the Lung Tissue: May Acetylsalicylic Acid Have a Positive Role?

    Science.gov (United States)

    Demirel, Can; Kilciksiz, Sevil Cagiran; Gurgul, Serkan; Erdal, Nurten; Yigit, Seyran; Tamer, Lulufer; Ayaz, Lokman

    2016-02-01

    The lung is relatively sensitive to irradiation. It is shown that acetylsalicylic acid (ASA) might reduce oxidative injury and that it has a place in protection from cancer. The aim of this study is to evaluate the potential radioprotective effects of ASA. Whole-body irradiation (6 Gy, single dose) was applied to the rats. Glutathione (GSH), malondialdehyde (MDA), myeloperoxidase (MPO), and nitric oxide (NO) levels in the lung tissue were measured. Control (C), Radiation (R), Radiation + ASA (R + ASA; received irradiation and 25 mg/kg of ASA intraperitoneally (i.p.)), and Radiation + Amifostine (R + WR-2721; received irradiation and 200 mg/kg of WR-2721 i.p.) groups were used. The MPO levels decreased statistically significantly in the group administered ASA. Histopathologically, a radioprotective effect of ASA was more evident in the R + ASA group. ASA is an agent which has not been used as a radioprotector in the clinic yet, and it is worth supporting with more advanced studies.

  14. The infrared spectra and structure of acetylsalicylic acid (aspirin) and its oxyanion: an ab initio force field treatment

    Science.gov (United States)

    Binev, I. G.; Stamboliyska, B. A.; Binev, Y. I.

    1996-05-01

    The structures of acetylsalicylic acid (aspirin) (I) and its oxyanion (II) have been studied by means of infrared spectra and ab initio 3-21 G force field calculations. The 3100-1100 cm -1 region bands of both the aspirin molecule and its oxyanion have been assigned. The theoretical infrared data for the free aspirin anion are in good agreement with the experimental data for aspirin alkali-metal salts in dimethyl sulfoxide- d6. The theoretical geometrical parameters for the isolated aspirin molecule are close to the literature X-ray diffraction data for its dimer in the solid state, except for those of the carboxy group, which participates directly in hydrogen bond formation. The changes in both the spectral and geometrical parameters, caused by the conversion of the aspirin molecule into the anion, are essential, but they are localized mainly within the carboxy group and the adjacent C-Ph bond. This is also true for the changes in the corresponding bond indices and electronic charges.

  15. Experimental research on synthesis of acetylsalicylic acid by miniaturization methods%乙酰水杨酸微型化合成实验研究

    Institute of Scientific and Technical Information of China (English)

    曾琦斐

    2011-01-01

    探讨乙酰水杨酸微型化合成的最佳实验条件.以浓硫酸作催化剂,用乙酸酐与水杨酸进行酰化反应制备乙酰水杨酸,改变反应条件进行实验,重点考察了反应物摩尔数比、反应温度、反应时间及催化剂等条件对反应的影响.乙酰水杨酸微型化合成的最佳实验条件是:乙酸酐和水杨酸的摩尔数比为3:1,反应温度60~80℃,以浓硫酸作催化剂,反应时间3~5 min.%The best experimental conditions of synthesis of acetylsalicylic acid by miniaturization methods were studies.The acetylsalicylic acid was synthesized from the salicylic acid and acetic anhydrode through acetoxylation, which takes the strong sulfuric acid as catalysis.Experiments were carried out under different conditions.The effect of molar ratio,reaction temperature,reaction time and catalyst on reaction were discussed.The best experiment conditions of synthesis of acetylsalicylic acid by miniaturization methods are:the optimum molar ratio of acetic anhydride to salicylic acid is 3 ∶ 1 ,the best reaction temperature is 60 ~80 ℃,taking the strong sulfuric acid as catalyst,the best reaction time is 3 ~5 min.

  16. The role of trefoil factor family in apparently healthy subjects administrated gastroprotective agents for the primary prevention of gastrointestinal injuries from low-dose acetylsalicylic acid: a preliminary study.

    Science.gov (United States)

    Kawai, Takashi; Takagi, Yu; Fukuzawa, Mari; Yamagishi, Tetsuya; Goto, Shinya

    2011-09-01

    It is well-known that acetylsalicylic acid induces gastrointestinal complication. Recently, trefoil factor family has been reported as a mucosal protective factor. We focused on trefoil factor family as one of defensive system for gastrointestinal injuries. The aim of this trial was to evaluate trefoil factor family levels in the serum of healthy subjects with low-dose acetylsalicylic acid. Low-dose acetylsalicylic acid with placebo or proton pump inhibitor or rebamipide were administered in 30 healthy subjects. Transnasal endoscopy was performed at 0, 24 h, 3 and 7 day. Changing of trefoil factor family (1,2,3) and numbers of gastric injuries were evaluated. The numbers of gastric injuries were significantly increased in the placebo group at 3 and 7 days. Injuries in the proton pump inhibitor group were not induced, in the rebamipide group were slightly induced. Trefoil factor family level in the placebo group were decreased in 3 and 7 days compared with prior to starting the trial. Trefoil factor family may have an important association with acetylsalicylic acid-induced gastrointestinal damage. Proton pump inhibitor and rebamipide prevented low-dose acetylsalicylic acid-induced gastrointestinal complications compared with the placebo group.

  17. Pharmacokinetic study of a new oral buffered acetylsalicylic acid (ASA) formulation in comparison with plain ASA in healthy volunteers.

    Science.gov (United States)

    Viganò, G; Garagiola, U; Gaspari, F

    1991-01-01

    A single-blind, randomized, crossover pharmacokinetic study was carried out to investigate the bioavailability of a new oral buffered 325 mg acetylsalicylic acid (ASA) formulation (ASPIRINA 03) in comparison with a 325 mg plain tablet. Twelve healthy volunteers of both sexes, aged between 20 and 37 years, received buffered or plain ASA on two separate occasions with a wash-out interval of at least two weeks. ASA and salicylic acid (SA) plasma levels were determined by a chromatographic method. The results showed no difference between the area under concentration time curve (AUC0-infinity) ASA values of both formulations (p = 0.19), and buffered ASA relative bioavailability was 102.49% (= bioequivalence). A significant difference was found between the AUC0-30 min ASA values: 90.5 micrograms. min/ml with buffered and 67.7 micrograms. min/ml with the plain tablet (p less than 0.05). The buffered ASA time of maximum concentration was shorter (28 +/- 8 min) than the plain one (38 +/- 19 min, p less than 0.05). The plasma concentrations and pharmacokinetic parameters of SA were not significantly different after the administration of the two ASA formulations. The plain ASA tablet had a significantly lower (p less than 0.05) dissolution rate than buffered ASA tablet. Moreover, the buffered ASA tablet significantly (p less than 0.01) increased the pH by 0.5 units. In conclusion, the bioavailability of the new oral buffered ASA was equivalent to that of plain ASA, but the plasma concentration peak was reached in a shorter time.

  18. Synthesis of acetylsalicylic acid catalyzed by carbon-based solid acid%碳基固体酸催化合成乙酰水杨酸

    Institute of Scientific and Technical Information of China (English)

    占昌朝; 曹小华; 严平; 王剑波; 余祖进; 江小平

    2012-01-01

    Carbon-based solid acid catalysts synthesized from starch andp-toluene sulphonic acid were characterized by FTIR, TG, BET, SEM and EDS. Its catalytic activity and effect of conventional heat and microwave heat on yield of acetylsalicylic acid were studied. The better condition was determined with single factor tests, which is as follows: the molar ratio of acetic anhydride to salicylic acid was 1.5 : 1, the weight ratio of carbon-based solid acid to salicylic acid was 5.8%, acylation reaction temperature was 76--80 ~C, reaction time was 25 min under conventional heat. The yield of acetylsalicylic acid was 82.1% and kept 78.2% after used five times under conventional heat. The carbon-based solid acid catalyst has high catalytic activity and retrievability under conventional heat, which are better than that of microwave heat.%以淀粉和对甲苯磺酸为原料合成了碳基固体酸催化剂,并采用FTIR、TG、BET、SEM和EDS对催化剂进行了表征。研究了催化剂对乙酰水杨酸合成反应的催化活性,并比较了常规加热和微波加热方式对反应的影响。通过单因素试验确定了较佳工艺条件为:乙酸酐与水杨酸物质的量比为1.5∶1,催化剂用量为水杨酸质量的5.8%,反应时间25 min,反应温度76~80℃。常规加热条件下收率82.1%,使用5次后,收率仍保持在78.2%。碳基固体酸催化剂在常规加热条件下催化性能和重复使用性能均优于微波加热条件反应。

  19. Next-generation re-sequencing of genes involved in increased platelet reactivity in diabetic patients on acetylsalicylic acid.

    Science.gov (United States)

    Postula, Marek; Janicki, Piotr K; Eyileten, Ceren; Rosiak, Marek; Kaplon-Cieslicka, Agnieszka; Sugino, Shigekazu; Wilimski, Radosław; Kosior, Dariusz A; Opolski, Grzegorz; Filipiak, Krzysztof J; Mirowska-Guzel, Dagmara

    2016-06-01

    The objective of this study was to investigate whether rare missense genetic variants in several genes related to platelet functions and acetylsalicylic acid (ASA) response are associated with the platelet reactivity in patients with diabetes type 2 (T2D) on ASA therapy. Fifty eight exons and corresponding introns of eight selected genes, including PTGS1, PTGS2, TXBAS1, PTGIS, ADRA2A, ADRA2B, TXBA2R, and P2RY1 were re-sequenced in 230 DNA samples from T2D patients by using a pooled PCR amplification and next-generation sequencing by Illumina HiSeq2000. The observed non-synonymous variants were confirmed by individual genotyping of 384 DNA samples comprising of the individuals from the original discovery pools and additional verification cohort of 154 ASA-treated T2DM patients. The association between investigated phenotypes (ASA induced changes in platelets reactivity by PFA-100, VerifyNow and serum thromboxane B2 level [sTxB2]), and accumulation of rare missense variants (genetic burden) in investigated genes was tested using statistical collapsing tests. We identified a total of 35 exonic variants, including 3 common missense variants, 15 rare missense variants, and 17 synonymous variants in 8 investigated genes. The rare missense variants exhibited statistically significant difference in the accumulation pattern between a group of patients with increased and normal platelet reactivity based on PFA-100 assay. Our study suggests that genetic burden of the rare functional variants in eight genes may contribute to differences in the platelet reactivity measured with the PFA-100 assay in the T2DM patients treated with ASA.

  20. Effects of nimesulide, acetylsalicylic acid, ibuprofen and nabumetone on cyclooxygenase-1- and cyclooxygenase-2-mediated prostanoid production in healthy volunteers ex vivo.

    Science.gov (United States)

    Kerola, Markku; Vuolteenaho, Katriina; Kosonen, Outi; Kankaanranta, Hannu; Sarna, Seppo; Moilanen, Eeva

    2009-01-01

    : The beneficial actions of non-steroidal anti-inflammatory drugs (NSAIDs) have been associated with inhibition of cyclooxygenase-2 (COX-2), whereas some of their adverse effects are associated mainly with inhibition of COX-1. Selective COX-2 inhibitors reduce the risk of gastrointestinal adverse events, but increase the risk of thromboembolic events pointing to importance of optimal COX-1/COX-2 inhibition in drug safety. We compared the effects of acetylsalicylic acid, ibuprofen, nabumetone and nimesulide on COX-1 and COX-2 pathways in healthy volunteers in an ex vivo set-up using single oral doses commonly used to treat acute pain. In a randomized, double-blind four-phase cross-over study, 15 healthy volunteers were given orally a single dose of either acetylsalicylic acid 500 mg, ibuprofen 400 mg, nabumetone 1 g or nimesulide 100 mg. Blood samples were drawn before and 1, 3, 6, 24 and 48 hr after the drug for the assessment of COX-1 and COX-2 activity. COX-1 activity was measured as thromboxane(2) production during blood clotting and COX-2 activity as endotoxin-induced prostaglandin E(2) synthesis in blood leucocytes. The data show that after a single oral dose these four NSAIDs have different profiles of action on COX-1 and COX-2. As expected, acetylsalicylic acid appeared to be COX-1-selective and ibuprofen effectively inhibited both COX-1 and COX-2. Nabumetone showed only a slight inhibitory effect on COX-1 and COX-2. Nimesulide caused almost complete suppression of COX-2 activity and a partial reduction of COX-1 activity. This confirms the relative COX-2 selectivity of nimesulide.

  1. Promoting endothelial recovery and reducing neointimal hyperplasia using sequential-like release of acetylsalicylic acid and paclitaxel-loaded biodegradable stents

    Directory of Open Access Journals (Sweden)

    Lee CH

    2014-08-01

    Full Text Available Cheng-Hung Lee,1,2 Chia-Ying Yu,2 Shang-Hung Chang,1 Kuo-Chun Hung,1 Shih-Jung Liu,2 Chao-Jan Wang,3 Ming-Yi Hsu,3 I-Chang Hsieh,1 Wei-Jan Chen,1 Yu-Shien Ko,1 Ming-Shien Wen1 1Division of Cardiology, Department of Internal Medicine, Chang Gung Memorial Hospital-Linkou, Tao-Yuan, Taiwan; 2Department of Mechanical Engineering, Chang Gung University, Tao-Yuan, Taiwan; 3Department of Medical Imaging and Intervention, Chang Gung Memorial Hospital, Linkou, Tao-Yuan, Taiwan Introduction: This work reports on the development of a biodegradable dual-drug-eluting stent with sequential-like and sustainable drug-release of anti-platelet acetylsalicylic acid and anti-smooth muscle cell (SMC proliferative paclitaxel.Methods: To fabricate the biodegradable stents, poly-L-lactide strips are first cut from a solvent-casted film. They are rolled onto the surface of a metal pin to form spiral stents. The stents are then consecutively covered by acetylsalicylic acid and paclitaxel-loaded polylactide-polyglycolide nanofibers via electrospinning.Results: Biodegradable stents exhibit mechanical properties that are superior to those of metallic stents. Biodegradable stents sequentially release high concentrations of acetylsalicylic acid and paclitaxel for more than 30 and 60 days, respectively. In vitro, the eluted drugs promote endothelial cell numbers on days 3 and 7, and reduce the proliferation of SMCs in weeks 2, 4, and 8. The stents markedly inhibit the adhesion of platelets on days 3, 7, and 14 relative to a non-drug-eluting stent. In vivo, the implanted stent is intact, and no stent thrombosis is observed in the stent-implanted vessels without the administration of daily oral acetylsalicylic acid. Promotion of endothelial recovery and inhibition of neointimal hyperplasia are also observed on the stented vessels.Conclusion: The work demonstrates the efficiency and safety of the biodegradable dual-drug-eluting stents with sequential and sustainable drug release

  2. Quantification of ascorbic acid and acetylsalicylic acid in effervescent tablets by CZE-UV and identification of related degradation products by heart-cut CZE-CZE-MS.

    Science.gov (United States)

    Neuberger, Sabine; Jooß, Kevin; Ressel, Christian; Neusüß, Christian

    2016-12-01

    Capillary electrophoresis is commonly applied for the analysis of pharmaceutical products due to its high separation efficiency and selectivity. For this purpose, electrospray-ionization-(ESI)-interfering additives or electrolytes are often required, which complicates the identification of impurities and degradation products by mass spectrometry (MS). Here, a capillary zone electrophoresis (CZE) method with ultraviolet (UV) absorption detection for the simultaneous determination and quantification of ascorbic acid and acetylsalicylic acid in effervescent tablets was developed. Related degradation products were identified via CZE-CZE-MS. Systematic optimization yielded 100 mM tricine (pH = 8.8) as appropriate background electrolyte, resulting in baseline separation of ascorbic acid, acetylsalicylic acid, and related anionic UV-active degradation products. The CZE-UV method was successfully validated regarding the guidelines of the Food and Drug Administration. The validated method was applied to trace the degradation rate of the active pharmaceutical ingredients at defined ambient conditions. A heart-cut CZE-CZE-MS approach, including a 4-port-nL-valve, was performed for the identification of the observed degradation products. This 2D setup enables a precise cutting of accurate sample volumes (20 nL) and the independent operation of two physically separated CZE dimensions, which is especially beneficial regarding MS detection. Hence, the ESI-interfering tricine electrolyte components were separated from the analytes in a second electrophoretic dimension prior to ESI-MS detection. The degradation products were identified as salicylic acid and mono- and diacetylated ascorbic acid. This setup is expected to be generally applicable for the mass spectrometric characterization of CZE separated analytes in highly ESI-interfering electrolyte systems. Graphical Abstract A CZE-UV method for the quantification of effervescent tablet ingredients and degradation products

  3. Rapid and sensitive determination of acetylsalicylic acid and salicylic acid in plasma using liquid chromatography-tandem mass spectrometry: application to pharmacokinetic study.

    Science.gov (United States)

    Xu, Xiangrong; Koetzner, Lee; Boulet, Jamie; Maselli, Harry; Beyenhof, Jessica; Grover, Gary

    2009-09-01

    A simple and sensitive analytical method using liquid chromatography-tandem mass spectrometry (LC/MS/MS) for determination of acetylsalicylic acid (aspirin, ASA) and its major metabolite, salicylic acid (SA), in animal plasma has been developed and validated. Both ASA and SA in plasma samples containing potassium fluoride were extracted using acetonitrile (protein precipitation) with 0.1% formic acid in it. 6-Methoxysalicylic acid was used as the internal standard (IS). The compounds were separated on a reversed-phase column. The multiple reaction monitoring mode was used with ion transitions of m/z 178.9 --> 136.8, 137.0 --> 93.0 and 167.0 --> 123.0 for ASA, SA and IS, respectively. The lower limits of quantification for ASA and SA were 3 and 30 ng/mL, respectively. The developed method was successfully applied for the evaluation of pharmacokinetics of ASA and SA after p.o. and i.v. administration of 1 mg/kg to rats.

  4. Inhibition of aberrant complement activation by a dimer of acetylsalicylic acid.

    Science.gov (United States)

    Lee, Moonhee; Wathier, Matthew; Love, Jennifer A; McGeer, Edith; McGeer, Patrick L

    2015-10-01

    We here report synthesis for the first time of the acetyl salicylic acid dimer 5,5'-methylenebis(2-acetoxybenzoic acid) (DAS). DAS inhibits aberrant complement activation by selectively blocking factor D of the alternative complement pathway and C9 of the membrane attack complex. We have previously identified aurin tricarboxylic and its oligomers as promising agents in this regard. DAS is much more potent, inhibiting erythrocyte hemolysis by complement-activated serum with an IC50 in the 100-170 nanomolar range. There are numerous conditions where self-damage from the complement system has been implicated in the pathology, including such chronic degenerative diseases of aging as Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis, and age-related macular degeneration. Consequently, there is a high priority for the discovery and development of agents that can successfully treat such conditions. DAS holds considerable promise for being such an agent.

  5. Administration of zinc complex of acetylsalicylic acid after the onset of myocardial injury protects the heart by upregulation of antioxidant enzymes.

    Science.gov (United States)

    Korkmaz-Icöz, Sevil; Atmanli, Ayhan; Radovits, Tamás; Li, Shiliang; Hegedüs, Peter; Ruppert, Mihály; Brlecic, Paige; Yoshikawa, Yutaka; Yasui, Hiroyuki; Karck, Matthias; Szabó, Gábor

    2016-03-01

    We recently demonstrated that the pre-treatment of rats with zinc and acetylsalicylic acid complex in the form of bis(aspirinato)zinc(II) [Zn(ASA)2] is superior to acetylsalicylic acid in protecting the heart from acute myocardial ischemia. Herein, we hypothesized that Zn(ASA)2 treatment after the onset of an acute myocardial injury could protect the heart. The rats were treated with a vehicle or Zn(ASA)2 after an isoproterenol injection. Isoproterenol-induced cardiac damage [inflammatory infiltration into myocardial tissue, DNA-strand breakage evidenced by TUNEL-assay, increased 11-dehydro thromboxane (TX)B2-levels, elevated ST-segment, widened QRS complex and prolonged QT-interval] was prevented by the Zn(ASA)2 treatment. In isoproterenol-treated rats, load-independent left ventricular contractility parameters were significantly improved after Zn(ASA)2. Furthermore, Zn(ASA)2 significantly increased the myocardial mRNA-expression of superoxide dismutase-1, glutathione peroxidase-4 and decreased the level of Na(+)/K(+)/ATPase. Postconditioning with Zn(ASA)2 protects the heart from acute myocardial ischemia. Its mechanisms of action might involve inhibition of pro-inflammatory prostanoids and upregulation of antioxidant enzymes.

  6. [Ability to Overcome the Thrombocyte Resistance to Acetylsalicylic Acid in Patients With Coronary Artery Disease After Myocardial Revascularization With Coronary Stenting].

    Science.gov (United States)

    Pershukov, I V; Ostaschenko, S L; Kuznetsova, T N; Scherbo, S N; Karben, Z A; Sokryukina, E V; Omarov, A A; Ramazanov, D M; Bosak, N V; Shulzhenko, L V; Kalmatov, R K; Batyraliev, T A; Sidorenko, B A

    2016-07-01

    Resistance to acetylsalicylic acid (ASA) in patients with coronary artery disease is a poor predictor for the development of atherothrombotic complications. In 277 patients with coronary artery disease suffered uncomplicated coronary angioplasty with stent implantation, we was estimated arachidon-induced platelet aggregation during treatment with acetylsalicylic acid by bedside VerifyNow Assay test at 28-90 days after the intervention. It was found that 18.9% of the 144 patients receiving a combination of ASA 75 mg with 15.2 mg of magnesium hydroxide had true (laboratory) resistance to ASA. At the same time on the original enteric coated ASA 100 mg, we can found only 0.8% resistance to ASA among 129 patients. We made switch from combination of ASA 75 mg with 15.2 mg of magnesium hydroxide to original enteric coated ASA 100 mg and repeat VerifyNow Assay test at 2-4 days and found lost of resistance in 92% of 28 patients. Thus, resistance to the ASA is not constant, it depends on the form and the applied dose of ASA, and eliminating more than 92% when ASA changes from ineffective to effective form.

  7. [Platelet aggregation upon acetylsalicylic acid and clopidogrel treatment and glycoprotein IIb/IIIa content in patients with acute coronary syndrome].

    Science.gov (United States)

    Khaspekova, S G; Ziuriaev, I T; Iakushkin, V V; Golubeva, N V; Ruda, M Ia; Mazurov, A V

    2011-01-01

    Interaction between aggregating activity of platelets and glycoprotein (GP) IIb/IIIa (fibrinogen receptor) content on their surface was investigated in patients with acute coronary syndrome (ACS). Eighty nine ACS patients were included into the study - 69 with and 20 without elevation of ST segment. Blood was collected within the first hour of admission to the clinic (1 day), and then at 3-5 and 8-12 days. All patients received standard antiaggregant therapy - acetylsalicylic acid - ASA (thromboxane A2 synthesis inhibitor) and clopidogrel (ADP receptor antagonist). Platelet aggregation was analyzed at the first time point when patients had already taken ASA but not clopidogrel, and then (3-5 and 8- 12 days) upon combined therapy with both preparations. Aggregation was induced by 5 and 20 uM ADP and measured by turbidimetric method. In comparison with the initial level (1 day, ASA) at days 3-5, i.e. after development of clopidogrel effect, platelet aggregation was decreased by 54 and 40% upon its stimulation with 5 and 20 uM ADP, and was not further changed at days 8-12. GP IIb/IIIa content on platelet surface was determined by binding of 125I-labelled monoclonal antibody CRC64. GP IIb/IIIa number varied from 31100 to 73000 per platelet with the mean level of 48500 +/- 8400 (mean +/- standard deviation). No differences were detected between mean GP IIb/IIIa number at 1, 3-5 and 8-12 days after ACS onset. Upon repeat GP IIb/IIIa measurement coefficient of variation was 6.1% demonstrating the stability of this parameter in each patient. Positive correlation between platelet aggregation and GP IIb/IIIa content was detected at the first day - correlation coefficients (r) 0.425 and 0.470 for 5 and 20 uM ADP (n=57, p0.05). These results indicates that variations of GP IIb/IIIa content affect platelet aggregating activity within first hours of ACS upon ASA treatment. However after saturation with clopidogrel this factor has no significant influence on platelet aggregation

  8. Acetylsalicylic acid (aspirin) and salicylic acid interaction with the human erythrocyte membrane bilayer induce in vitro changes in the morphology of erythrocytes.

    Science.gov (United States)

    Suwalsky, Mario; Belmar, Jessica; Villena, Fernando; Gallardo, María José; Jemiola-Rzeminska, Malgorzata; Strzalka, Kazimierz

    2013-11-01

    Despite the well-documented information, there are insufficient reports concerning the effects of salicylate compounds on the structure and functions of cell membranes, particularly those of human erythrocytes. With the aim to better understand the molecular mechanisms of the interaction of acetylsalicylic acid (ASA) and salicylic acid (SA) with cell membranes, human erythrocyte membranes and molecular models were utilized. These consisted of bilayers of dimyristoylphosphatidylcholine (DMPC) and dimyristoylphosphatidylethanolamine (DMPE), representative of phospholipid classes located in the outer and inner monolayers of the human erythrocyte membrane, respectively. The capacity of ASA and SA to perturb the multibilayer structures of DMPC and DMPE was evaluated by X-ray diffraction while DMPC unilamellar vesicles (LUV) were studied by fluorescence spectroscopy. Moreover, we took advantage of the capability of differential scanning calorimetry (DSC) to detect the changes in the thermotropic phase behavior of lipid bilayers resulting from ASA and SA interaction with PC and PE molecules. In an attempt to further elucidate their effects on cell membranes, the present work also examined their influence on the morphology of intact human erythrocytes by means of defocusing and scanning electron microscopy, while isolated unsealed human erythrocyte membranes (IUM) were studied by fluorescence spectroscopy. Results indicated that both salicylates interact with human erythrocytes and their molecular models in a concentration-dependent manner perturbing their bilayer structures.

  9. Development of a new analytical method for determination of acetylsalicylic and salicylic acids in tablets by reversed phase liquid chromatography

    Directory of Open Access Journals (Sweden)

    José Luiz Neves de Aguiar

    2009-12-01

    Full Text Available Acetylsalicylic acid (AAS is a drug utilized as analgesic, anti-inflammatory, and antipyretic medication, available worldwide and commonly used in Brazil. Salicylic acid (AS is a precursor in AAS synthesis and is also produced during its degradation. The official United States Pharmacopoeia (USP suggests the determination of these drugs by high performance liquid chromatography (HPLC, with ultraviolet detection, but this method has neither a high sensitivity (S AAS=0.12 mAbs/(μg/mL and S AS=0.48 mAbs/(μg/mL nor resolution (Rs=1.61. The purpose of this study was to develop a new more adequate, accurate method by liquid phase chromatography than the current official methodology, and to use this new method in the determination of the tenors of acetylsalicylic, as of salicylic acids in tablets. The parameters of the chromatographic system for both the AAS and AS were satisfactory. Selectivity was verified by absorption spectra comparison in the ultraviolet (UV range, during and after substance retention time. The linear range for AAS was 0.21 to 0.39 mg/mL, and that for AS was 6.3 to 11.7 μg/mL. The correlation coefficients (r of the analytical curves of AAS and AS were 0.9995 and 0.9988, respectively; and the detection and quantification limits for the AS were 0.23 and 0.69 μg/mL. The sensitivity (S AAS=1.88 mAbs/(μg/mL and S AS=1.84 mAbs/(μg/mL and the resolution (Rs =5.06 show the improvement obtained using this method over that described by the USP.O ácido acetilsalicílico (AAS é um fármaco utilizado como analgésico, antiinflamatório, antipirético, sendo amplamente comercializado e consumido no Brasil e no mundo. Como precursor de sua síntese utiliza-se o ácido salicílico (AS que também é produzido através de sua degradação. A metodologia oficial da Farmacopéia Americana (USP preconiza a determinação destes fármacos por cromatografia líquida de alta eficiência (CLAE com detecção por ultravioleta, mas este método n

  10. 合成乙酰水杨酸的反应条件的探讨%Research of Reaction Conditions about Acetylsalicylic Acid Synthesized

    Institute of Scientific and Technical Information of China (English)

    李娅生; 刘大勇; 王九; 王昱航; 陈强; 付富生

    2012-01-01

    对乙酰水杨酸“老药新用”的应用现状以及应用前景进行了详细的分析。比较了目前市场上乙酰水杨酸各种合成方法的优劣,设计了适合于工业化的较佳的合成路线,考察了原料物质的量之比、催化剂用量、反应温度、反应时间对反应收率的影响,进一步优化了合成工艺。经过实验数据的处理与分析,采用O-酰基化反应合成乙酰水杨酸的适宜条件为:无水环境下,对甲苯磺酸为催化剂,n(水杨酸):n(乙酸酹)=1:2.0:反应温度为85℃和反应时间为30rain时,乙酰水杨酸的收率高于97%。所得样品符合《中国药典》和《美国药典》中乙酰水杨酸的质量要求,能够用于合成乙酰水杨酸。%Acetylsalicylic acid "new use for an old drug" application status and application prospect were analyzed in detail. Compared with the present market of acetylsalicylic acid synthesis methods advantages and disadvantages. Design suitable for industrialization of better synthetic route. The effect of raw material ratio, the dosage of catalyst, reaction temperature, reaction time on the yield of the reaction, further optimization of the synthesis technology. Through the experimental data processing and analysis, the O acylation reaction conditions for synthesis of acetyl salicylic acid: without water environment, concentrated 4-Toluene sulfonic acid as catalyst, n(salicylic acid) " n(acetic anhydride)=l : 2.0; when the reaction temperature of 85 ℃ and reaction time of 30 min, acetyl salicylic acid yield were higher than 97 %. The sample meets acetylsalicylic acid quality requirements of"Chinese Pharmacopoeia" and "with the United States Pharmacopoeia", can be used for the synthesis of acetyl salicylic acid.

  11. Modulation of phenytoin teratogenicity and embryonic covalent binding by acetylsalicylic acid, caffeic acid, and alpha-phenyl-N-t-butylnitrone: implications for bioactivation by prostaglandin synthetase

    Energy Technology Data Exchange (ETDEWEB)

    Wells, P.G.; Zubovits, J.T.; Wong, S.T.; Molinari, L.M.; Ali, S.

    1989-02-01

    Teratogenicity of the anticonvulsant drug phenytoin is thought to involve its bioactivation by cytochromes P-450 to a reactive arene oxide intermediate. We hypothesized that phenytoin also may be bioactivated to a teratogenic free radical intermediate by another enzymatic system, prostaglandin synthetase. To evaluate the teratogenic contribution of this latter pathway, an irreversible inhibitor of prostaglandin synthetase, acetylsalicylic acid (ASA), 10 mg/kg intraperitoneally (ip), was administered to pregnant CD-1 mice at 9:00 AM on Gestational Days 12 and 13, 2 hr before phenytoin, 65 mg/kg ip. Other groups were pretreated 2 hr prior to phenytoin administration with either the antioxidant caffeic acid or the free radical spin trapping agent alpha-phenyl-N-t-butylnitrone (PBN). Caffeic acid and PBN were given ip in doses that respectively were up to 1.0 to 0.05 molar equivalents to the dose of phenytoin. Dams were killed on Day 19 and the fetuses were assessed for teratologic anomalies. A similar study evaluated the effect of ASA on the in vivo covalent binding of radiolabeled phenytoin administered on Day 12, in which case dams were killed 24 hr later on Day 13. ASA pretreatment produced a 50% reduction in the incidence of fetal cleft palates induced by phenytoin (p less than 0.05), without significantly altering the incidence of resorptions or mean fetal body weight. Pretreatment with either caffeic acid or PBN resulted in dose-related decreases in the incidence of fetal cleft palates produced by phenytoin, with maximal respective reductions of 71 and 82% at the highest doses of caffeic acid and PBN (p less than 0.05).

  12. Effects of paracetamol, non-steroidal anti-inflammatory drugs, acetylsalicylic acid, and opioids on bone mineral density and risk of fracture: results of the Danish Osteoporosis Prevention Study (DOPS)

    DEFF Research Database (Denmark)

    Vestergaard, Peter; Hermann, P; Jensen, J-E B

    2012-01-01

    Pain medication has been associated with fractures. We found higher weight in paracetamol and non-steroidal anti-inflammatory drugs (NSAID) users and lower vitamin D levels in opioid and acetylsalicylic acid users. None of the pain medications influenced bone mineral density or loss. NSAID were...

  13. Raman spectroscopy and capillary zone electrophoresis for the analysis of degradation processes in commercial effervescent tablets containing acetylsalicylic acid and ascorbic acid.

    Science.gov (United States)

    Neuberger, Sabine; Jooß, Kevin; Flottmann, Dirk; Scriba, Gerhard; Neusüß, Christian

    2017-02-05

    In order to ensure the stability of pharmaceutical products appropriate manufacturing and storage conditions are required. In general, the degradation of active pharmaceutical ingredients (APIs) and subsequent formation of degradation products affect the pharmaceutical quality. Thus, a fast and effective detection and characterization of these substances is mandatory. Here, the applicability of Raman spectroscopy and CZE for the characterization of the degradation of effervescent tablets containing acetylsalicylic acid (ASA) and ascorbic acid (AA) was evaluated. Therefore, a degradation study was performed analyzing tablets from two different manufacturers at varying conditions (relative humidity (RH) 33%, 52% and 75% at 30°C). Raman spectroscopy combined with principal component analysis could be successfully applied for the fast and easy discrimination of non-degraded and degraded effervescent tablets after a storage period of approximately 24h (RH 52%). Nevertheless, a clear identification or quantification of APIs and degradation products within the analyzed tablets was not possible, i.a. due to missing reference materials. CZE-UV enabled the quantification of the APIs (ASA, AA) and related degradation products (salicylic acid (SA); semi-quantitative also mono- and diacetylated AA) within the complex tablet mixtures. The higher the RH, the faster the degradation of ASA and AA as well as the formation of the degradation products. Mono- and diacetylated AA are major primary degradation products of AA for the applied effervescent tablets. A significant degradation of the APIs was detected earlier by CZE (6-12h, RH 52%) than by Raman spectroscopy. Summarized, Raman spectroscopy is well-suited as quick test to detect degradation of these tablets and CZE can be utilized for further detailed characterization and quantification of specific APIs and related degradation products.

  14. Antiplatelet Effect Durability of a Novel, 24-Hour, Extended-Release Prescription Formulation of Acetylsalicylic Acid in Patients With Type 2 Diabetes Mellitus.

    Science.gov (United States)

    Gurbel, Paul A; Bliden, Kevin P; Chaudhary, Rahul; Patrick, Jeff; Liu, Fang; Chen, Gailing; McLeod, Christopher; Tantry, Udaya S

    2016-12-15

    High platelet reactivity and high platelet turnover have been implicated in incomplete platelet inhibition during immediate-release acetylsalicylic acid therapy in patients with type 2 diabetes mellitus (DM). An extended-release acetylsalicylic acid (ER-ASA; Durlaza) formulation was developed to provide 24-hour antithrombotic effects with once-daily dosing. The objective of the study was to evaluate the antiplatelet effects of ER-ASA in patients with DM. In this open-label, single-center study, patients with DM (n = 40) and multiple cardiovascular risk factors received ER-ASA 162.5 mg/day for 14 ± 4 days. Multiple platelet function tests, serum and urinary thromboxane B2 metabolites, prostacyclin metabolite, and high-sensitive C-reactive protein levels were assessed at 1, 12, 16, and 24 hours post-dose. Patients with high platelet turnover and/or high platelet reactivity were treated with ER-ASA 325 mg/day for 14 ± 4 days, and laboratory analyses were repeated. All patients responded to ER-ASA 162.5 mg/day as measured by arachidonic acid-induced aggregation, and there was no loss of the platelet inhibitory effect of ER-ASA 162.5 mg/day over 24 hours post-dose (p = not significant). The antiplatelet effect was sustained over 24 hours for all platelet function measurements. Mean 1- to 24-hour serum thromboxane B2 levels were low with both doses and were lower with ER-ASA 325 mg/day compared with 162.5 mg/day therapy (p = 0.002). In conclusion, ER-ASA 162.5 mg daily dose provided sustained antiplatelet effects over 24 hours in patients with type 2 DM and multiple cardiovascular risk factors and had a favorable tolerability profile.

  15. A rapid method for the simultaneous determination of L-ascorbic acid and acetylsalicylic acid in aspirin C effervescent tablet by ultra performance liquid chromatography-tandem mass spectrometry

    Science.gov (United States)

    Wabaidur, Saikh Mohammad; Alothman, Zeid Abdullah; Khan, Mohammad Rizwan

    2013-05-01

    In present study, a rapid and sensitive method using ultra performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) was developed for the simultaneous determination of L-ascorbic acid and acetylsalicylic acid in aspirin C effervescent tablet. The optimum chromatographic separation was carried out on a reversed phase Waters® Acquity UPLC BEH C18 column (1.7 μm particle size, 100 mm × 2.1 mm ID) with an isocratic elution profile and mobile phase consisting of 0.1% formic acid in water and acetonitrile (75:25, v/v, pH 3.5) at flow rate of 0.5 mL min-1. The influences of mobile phase composition, flow rate and pH on chromatographic resolution were investigated. The total chromatographic analysis time was as short as 2 min with excellent resolution. Detection and quantification of the target compounds were carried out with a triple quadrupole mass spectrometer using negative electrospray ionization (ESI) and multiple reaction monitoring (MRM) modes. The performance of the method was evaluated and very low limits of detection less than 0.09 μg g-1, excellent coefficient correlation (r2 > 0.999) with liner range over a concentration range of 0.1-1.0 μg g-1 for both L-ascorbic acid and acetylsalicylic acid, and good intraday and interday precisions (relative standard deviations (R.S.D.) acid and acetylsalicylic acid in aspirin C effervescent tablet.

  16. Editorial on low-dose acetylsalicylic acid treatment and impact on short-term mortality in Staphylococcus aureus bloodstream infection: a propensity score-matched cohort study

    Science.gov (United States)

    Schoergenhofer, Christian; Schwameis, Michael; Lagler, Heimo

    2016-01-01

    The manuscript “Low-Dose Acetylsalicylic Acid Treatment and Impact on Short-Term Mortality in Staphylococcus aureus (S. aureus) Bloodstream Infection: A propensity Score-Matched Cohort Study” published in Critical Care Medicine by Osthoff et al. reported an association of aspirin intake with a reduced short-term mortality. Direct anti-microbial effects of aspirin and its metabolite salicylate were suggested in preclinical studies. Especially intriguing is the inclusion of a control group with Escherichia coli (E. coli) blood stream infections in this study, in which aspirin was not associated with an improved outcome. However, as other observational studies also reported benefits of aspirin in critically ill patients, randomized trials are needed to confirm the effects of low-dose aspirin. PMID:27294095

  17. The influence of dose, time of administration, body temperature and salicylate kinetics on the antithrombotic action of acetylsalicylic acid in male rats.

    Science.gov (United States)

    Philp, R B; Paul, M L; Killackey, J J; Killackey, B A

    1983-01-01

    Acetylsalicylic acid (ASA), given i.v. to male rats 10 min before electrical injury to the carotid artery, was found to reduce rate and extent of thrombosis at 3.3 and 10.0 mg/kg but not at 1.7, 20 or 100 mg/kg, indicating a narrow, low-dose window for antithrombotic effect. ASA was more effective in rats in which body temperature was allowed to fall greater than 0.5 degrees C but protection was lost if injury was delayed 15 min or more after ASA administration. Serum salicylate studies did not support the view that loss of protection was due to competition between salicylate and ASA for cyclooxygenase-binding sites. ASA was also protective at 200 mg/kg i.v., possibly through non-specific toxic effects.

  18. Cyclooxygenase product inhibition with acetylsalicylic acid slows disease progression in the Han:SPRD-Cy rat model of polycystic kidney disease.

    Science.gov (United States)

    Ibrahim, Naser H M; Gregoire, Melanie; Devassy, Jessay G; Wu, Yinhong; Yoshihara, Daisuke; Yamaguchi, Tamio; Nagao, Shizuko; Aukema, Harold M

    2015-01-01

    Renal cyclooxygenase (COX) derived eicosanoids are elevated and lipoxygenase (LOX) products are reduced in the Han:SPRD-Cy rat model of polycystic kidney disease (PKD). Selective COX2 inhibition reduces kidney disease progression, but COX1 levels also are elevated in this model. Since the effect of reducing the products of both COX isoforms and the role of LOX products is not known, weanling normal and diseased Han:SPRD-cy littermates were given either low dose acetylsalicylic acid (ASA), nordihydroguaiaretic (NDGA) or no treatment for eight weeks. Renal eicosanoids were altered in the diseased compared to normal cortex, with COX products being higher and LOX products being lower. ASA reduced COX products, cyst growth and kidney water content, while NDGA reduced LOX products without altering disease progression or kidney function. Hence, a human equivalent ASA dose equal to less than one regular strength aspirin per day slowed disease progression, while further reduction of LOX products did not worsen disease progression.

  19. Acetylsalicylic Acid reduces the severity of dextran sodium sulfate-induced colitis and increases the formation of anti-inflammatory lipid mediators.

    Science.gov (United States)

    Köhnke, Thomas; Gomolka, Beate; Bilal, Süleyman; Zhou, Xiangzhi; Sun, Yanping; Rothe, Michael; Baumgart, Daniel C; Weylandt, Karsten H

    2013-01-01

    The role of non-steroidal anti-inflammatory drugs in inflammatory bowel disease is controversial, as they have been implicated in disease aggravation. Different from other cyclooxygenase inhibitors, acetylsalicylic acid (ASA) enhances the formation of anti-inflammatory and proresolution lipoxins derived from arachidonic acid as well as resolvins from omega-3 polyunsaturated fatty acids such as docosahexaenoic acid (DHA). In this study, we examined the effect of ASA on murine dextran sodium sulfate colitis. A mouse magnetic resonance imaging (MRI) protocol and post mortem assessment were used to assess disease severity, and lipid metabolites were measured using liquid chromatography-coupled tandem mass spectrometry. Decreased colitis activity was demonstrated by phenotype and MRI assessment in mice treated with ASA, and confirmed in postmortem analysis. Analysis of lipid mediators showed sustained formation of lipoxin A4 and an increase of DHA-derived 17-hydroxydocosahexaenoic acid (17-HDHA) after treatment with ASA. Furthermore, in vitro experiments in RAW264.7 murine macrophages demonstrated significantly increased phagocytosis activity after incubation with 17-HDHA, supporting its proresolution effect. These results show a protective effect of ASA in a murine colitis model and could give a rationale for a careful reassessment of ASA therapy in patients with inflammatory bowel disease and particularly ulcerative colitis, possibly combined with DHA supplementation.

  20. Effects of the precalving administration of omega-3 fatty acids alone or in combination with acetylsalicylic acid in periparturient dairy cows.

    Science.gov (United States)

    Grossi, P; Bertoni, G; Cappelli, F Piccioli; Trevisi, E

    2013-06-01

    This study investigated the effects of the administration of long chain omega-3 fatty acids (ω-3 FA) and acetylsalicylic acid (ASA) on inflammation, performance, and fertility in periparturient dairy cows. Five weeks before calving, 26 multiparous dairy cows were randomly assigned to 1 of 3 treatments: ω-3 FA (n = 9; OME), ω-3 FA and ASA (n = 9; OMAS), or palm oil (n = 8; CTR). During the last 3 wk of pregnancy, OME and OMAS groups received daily 12.0 g of fish-derived ω-3 FA, whereas CTR cows received only SFA. In addition, OMAS cows received daily 6.0 mg ASA/kg BW starting at 7 d before calving. Only a few cows had health problems after calving, but those in OMAS were most affected (n = 3 vs. 1 in CTR). Inflammatory status around calving did not improve in OME cows, as confirmed by the patterns of concentration of acute-phase proteins (APP), which were similar to CTR. Compared with CTR and OME, the increase of the positive APP and the decrease of the negative APP (e.g., albumin; P < 0.01) observed in OMAS cows suggested a severe inflammatory status after calving. Compared with OMAS, postcalving energy metabolism was better in OME cows as shown by a lower degree of lipomobilization (smaller BCS drop, greater glucose) and milder ketogenesis (less β-hydroxybutyrate; P < 0.01). Cows in CTR had optimal fertility indices, whereas OMAS was the worst group. The severe inflammation and the more negative energy balance likely contributed to the poor fertility parameters in those cows. It is known that ASA exerts an inhibitory effect on cyclooxygenases, causing a possible decrease in the synthesis of PGF2α. A decreased concentration of PGF2α is connected with alterations in the physiologic processes related to labor and to uterine motility. Cows in OMAS had a longer pregnancy (P < 0.10 vs.OME) and a greater frequency of retained placenta, which may be attributed to decreased synthesis of PGF2α. The administration of ω-3 FA alone did not delay calving or the

  1. Simultaneous determination of salicylic, 3-methyl salicylic, 4-methyl salicylic, acetylsalicylic and benzoic acids in fruit, vegetables and derived beverages by SPME-LC-UV/DAD.

    Science.gov (United States)

    Aresta, Antonella; Zambonin, Carlo

    2016-03-20

    Salicylic and benzoic acid are phenolic acids occurring in plant cells, thus they can be present in fruit and vegetables at various levels. They possess anti-inflammatory and antimicrobial properties, however they may induce symptoms and health problems in a small percentage of the population. Therefore, a low phenolic acid diet may be of clinical benefit to such individuals. In order to achieve this goal, the concentration of these substances in different food and beverages should be assessed. The present work describes for the first time a new method, based on solid phase microextraction (polydimethylsiloxane-divinylbenzene fiber) coupled to liquid chromatography with UV diode array detection, for the simultaneous determination of salicylic acid, 3-methyl salicylic acid, 4-methyl salicylic acid, acetylsalicylic acid and benzoic acid in selected fruit, vegetables and beverages. All the aspects influencing fiber adsorption (time, temperature, pH, salt addition) and desorption (desorption and injection time, desorption solvent mixture composition) of the analytes have been investigated. An isocratic separation was performed using an acetonitrile-phosphate buffer (pH 2.8; 2 mM) mixture (70:30, v/v) as the mobile phase. The estimated LOD and LOQ values (μg/mL) were in the range 0.002-0.028 and 0.007-0.095. The within-day and day-to-day precision values (RSD%) were between 4.7-6.1 and 6.6-9.4, respectively. The method has been successfully applied to the analysis of fava beans, blueberries, kiwi, tangerines, lemons, oranges and fruit juice (lemon and blueberry) samples. The major advantage of the method is that it only requires simple homogenization and/or centrifugation and dilution steps prior to SPME and injection in the LC system.

  2. Bleeding and first-year mortality following hip fracture surgery and preoperative use of low-dose acetylsalicylic acid: an observational cohort study

    Directory of Open Access Journals (Sweden)

    Apelqvist Anna

    2011-11-01

    Full Text Available Abstract Background Hip fracture is associated with high mortality. Cardiovascular disease and other comorbidities requiring long-term anticoagulant medication are common in these mostly elderly patients. The objective of our observational cohort study of patients undergoing surgery for hip fracture was to study the association between preoperative use of low-dose acetylsalicylic acid (LdAA and intraoperative blood loss, blood transfusion and first-year all-cause mortality. Methods An observational cohort study was conducted on patients with hip fracture (cervical requiring hemiarthroplasty or pertrochanteric or subtrochanteric requiring internal fixation participating in a randomized trial that found lack of efficacy of a compression bandage in reducing postoperative bleeding. The participants were 255 patients (≥50 years of whom 118 (46% were using LdAA (defined as ≤320 mg daily preoperatively. Bleeding variables in patients with and without LdAA treatment at time of fracture were measured and blood transfusions given were compared using logistic regression. The association between first-year mortality and preoperative use of LdAA was analyzed with Cox regression adjusting for age, sex, type of fracture, baseline renal dysfunction and baseline cardiovascular and/or cerebrovascular disease. Results Blood transfusions were given postoperatively to 74 (62.7% LdAA-treated and 76 (54% non-treated patients; the adjusted odds ratio was 1.8 (95% CI 1.04 to 3.3. First-year mortality was significantly higher in LdAA-treated patients; the adjusted hazard ratio (HR was 2.35 (95% CI 1.23 to 4.49. The mortality was also higher with baseline cardiovascular and/or cerebrovascular disease, adjusted HR 2.78 (95% CI 1.31 to 5.88. Patients treated with LdAA preoperatively were significantly more likely to suffer thromboembolic events (5.7% vs. 0.7%, P = 0.03. Conclusions In patients with hip fracture (cervical treated with hemiarthroplasty or pertrochanteric

  3. The Influence of Prolonged Acetylsalicylic Acid Supplementation-Induced Gastritis on the Neurochemistry of the Sympathetic Neurons Supplying Prepyloric Region of the Porcine Stomach.

    Science.gov (United States)

    Palus, Katarzyna; Całka, Jarosław

    2015-01-01

    This experiment was designed to establish the localization and neurochemical phenotyping of sympathetic neurons supplying prepyloric area of the porcine stomach in a physiological state and during acetylsalicylic acid (ASA) induced gastritis. In order to localize the sympathetic perikarya the stomachs of both control and acetylsalicylic acid treated (ASA group) animals were injected with neuronal retrograde tracer Fast Blue (FB). Seven days post FB injection, animals were divided into a control and ASA supplementation group. The ASA group was given 100 mg/kg of b.w. ASA orally for 21 days. On the 28th day all pigs were euthanized with gradual overdose of anesthetic. Then fourteen-micrometer-thick cryostat sections were processed for routine double-labeling immunofluorescence, using primary antisera directed towards tyrosine hydroxylase (TH), dopamine β-hydroxylase (DβH), neuropeptide Y (NPY), galanin (GAL), neuronal nitric oxide synthase (nNOS), leu 5-enkephalin (LENK), cocaine- and amphetamine- regulated transcript peptide (CART), calcitonin gene-related peptide (CGRP), substance P (SP) and vasoactive intestinal peptide (VIP). The data obtained in this study indicate that postganglionic sympathetic nerve fibers supplying prepyloric area of the porcine stomach originate from the coeliac-cranial mesenteric ganglion complex (CCMG). In control animals, the FB-labelled neurons expressed TH (94.85 ± 1.01%), DβH (97.10 ± 0.97%), NPY (46.88 ± 2.53%) and GAL (8.40 ± 0.53%). In ASA group, TH- and DβH- positive nerve cells were reduced (85.78 ± 2.65% and 88.82 ± 1.63% respectively). Moreover, ASA- induced gastritis resulted in increased expression of NPY (76.59 ± 3.02%) and GAL (26.45 ± 2.75%) as well as the novo-synthesis of nNOS (6.13 ± 1.11%) and LENK (4.77 ± 0.42%) in traced CCMG neurons. Additionally, a network of CART-, CGRP-, SP-, VIP-, LENK-, nNOS- immunoreactive (IR) nerve fibers encircling the FB-positive perikarya were observed in both intact and ASA

  4. The Influence of Prolonged Acetylsalicylic Acid Supplementation-Induced Gastritis on the Neurochemistry of the Sympathetic Neurons Supplying Prepyloric Region of the Porcine Stomach.

    Directory of Open Access Journals (Sweden)

    Katarzyna Palus

    Full Text Available This experiment was designed to establish the localization and neurochemical phenotyping of sympathetic neurons supplying prepyloric area of the porcine stomach in a physiological state and during acetylsalicylic acid (ASA induced gastritis. In order to localize the sympathetic perikarya the stomachs of both control and acetylsalicylic acid treated (ASA group animals were injected with neuronal retrograde tracer Fast Blue (FB. Seven days post FB injection, animals were divided into a control and ASA supplementation group. The ASA group was given 100 mg/kg of b.w. ASA orally for 21 days. On the 28th day all pigs were euthanized with gradual overdose of anesthetic. Then fourteen-micrometer-thick cryostat sections were processed for routine double-labeling immunofluorescence, using primary antisera directed towards tyrosine hydroxylase (TH, dopamine β-hydroxylase (DβH, neuropeptide Y (NPY, galanin (GAL, neuronal nitric oxide synthase (nNOS, leu 5-enkephalin (LENK, cocaine- and amphetamine- regulated transcript peptide (CART, calcitonin gene-related peptide (CGRP, substance P (SP and vasoactive intestinal peptide (VIP. The data obtained in this study indicate that postganglionic sympathetic nerve fibers supplying prepyloric area of the porcine stomach originate from the coeliac-cranial mesenteric ganglion complex (CCMG. In control animals, the FB-labelled neurons expressed TH (94.85 ± 1.01%, DβH (97.10 ± 0.97%, NPY (46.88 ± 2.53% and GAL (8.40 ± 0.53%. In ASA group, TH- and DβH- positive nerve cells were reduced (85.78 ± 2.65% and 88.82 ± 1.63% respectively. Moreover, ASA- induced gastritis resulted in increased expression of NPY (76.59 ± 3.02% and GAL (26.45 ± 2.75% as well as the novo-synthesis of nNOS (6.13 ± 1.11% and LENK (4.77 ± 0.42% in traced CCMG neurons. Additionally, a network of CART-, CGRP-, SP-, VIP-, LENK-, nNOS- immunoreactive (IR nerve fibers encircling the FB-positive perikarya were observed in both intact and ASA

  5. Non-enzymatic modifications of prostaglandin H synthase 1 affect bifunctional enzyme activity - Implications for the sensitivity of blood platelets to acetylsalicylic acid.

    Science.gov (United States)

    Kassassir, Hassan; Siewiera, Karolina; Talar, Marcin; Stec-Martyna, Emilia; Pawlowska, Zofia; Watala, Cezary

    2016-06-25

    Due to its ability to inhibit the blood platelet PGHS-1, acetylsalicylic acid (ASA, Aspirin(®)) is widely used as a preventive agent in atherothrombotic diseases. However, its beneficial effects seem to be lower in diabetic patients, suggesting that protein glycation may impair effective ASA-mediated acetylation process. On the other hand, it is proposed that ASA can prevent some of the late complications of diabetes by lowering the extent of glycation at protein free amino groups. The aim of this work was to evaluate the extents of non-enzymatic N-glycosylation (glycation) and acetylation of blood platelet PGHS-1 (COX-1) and the competition between glycation and acetylation was investigated in order to demonstrate how these two reactions may compete against platelet PGHS-1. When PGHS-1 was incubated with glycating/acetylating agents (glucose, Glu; 1,6-bisphosphofructose, 1,6-BPF; methylglyoxal, MGO, acetylsalicylic acid, ASA), the enzyme was modified in 13.4 ± 1.6, 5.3 ± 0.5, 10.7 ± 1.2 and 6.4 ± 1.1 mol/mol protein, respectively, and its activity was significantly reduced. The prior glycation/carbonylation of PGHS-1 with Glu, 1,6-BPF or MGO decreased the extent of acetylation from 6.4 ± 1.1 down to 2.5 ± 0.2, 3.6 ± 0.3 and 5.2 ± 0.2 mol/mol protein, respectively, but the enzyme still remained susceptible to the subsequent inhibition of its activity with ASA. When PGHS-1 was first acetylated with ASA and then incubated with glycating/carbonylating agents, we observed the following reductions in the enzyme modifications: from 13.4 ± 1.6 to 8.7 ± 0.6 mol/mol protein for Glu, from 5.3 ± 0.5 to 3.9 ± 0.3 mol/mol protein for 1,6-BPF and from 10.7 ± 1.2 to 7.5 ± 0.5 mol/mol protein for MGO, however subsequent glycation/carbonylation did not significantly affect PGHS-1 function. Overall, our outcomes allow to better understand the structural aspects of the chemical competition between glycation and acetylation of PGHS-1.

  6. Probing of the combined effect of bisquaternary ammonium antimicrobial agents and acetylsalicylic acid on model phospholipid membranes: differential scanning calorimetry and mass spectrometry studies.

    Science.gov (United States)

    Kasian, N A; Pashynska, V A; Vashchenko, O V; Krasnikova, A O; Gömöry, A; Kosevich, M V; Lisetski, L N

    2014-12-01

    A model molecular biosystem of hydrated dipalmitoylphosphatidylcholine (DPPC) bilayers that mimics cell biomembranes is used to probe combined membranotropic effects of drugs by instrumental techniques of molecular biophysics. Differential scanning calorimetry reveals that doping of the DPPC model membrane with individual bisquaternary ammonium compounds (BQAC) decamethoxinum, ethonium, thionium and acetylsalicylic acid (ASA) leads to lowering of the membrane melting temperature (Tm) pointing to membrane fluidization. Combined application of the basic BQAC and acidic ASA causes an opposite effect on Tm (increase), corresponding to the membrane densification. Thus, modulation of the membranotropic effects upon combined use of the drugs studied can be revealed at the level of model membranes. Formation of noncovalent supramolecular complexes of the individual BQACs and ASA with DPPC molecules, which may be involved in the mechanism of the drug-membrane interaction at the molecular level, is demonstrated by electrospray ionization (ESI) mass spectrometry. In the ternary (DPPC + ASA + BQAC) model systems, the stable complexes of the BQAC dication with the ASA anion, which may be responsible for modulation of the membranotropic effects of the drugs, were recorded by ESI mass spectrometry. The proposed approach can be further developed for preliminary evaluation of the combined effects of the drugs at the level of model lipid membranes prior to tests on living organisms.

  7. Binary mixtures of diclofenac with paracetamol, ibuprofen, naproxen, and acetylsalicylic acid and these pharmaceuticals in isolated form induce oxidative stress on Hyalella azteca.

    Science.gov (United States)

    Gómez-Oliván, Leobardo Manuel; Neri-Cruz, Nadia; Galar-Martínez, Marcela; Islas-Flores, Hariz; García-Medina, Sandra

    2014-11-01

    Toxicity in natural ecosystems is usually not due to exposure to a single substance, but is rather the result of exposure to mixtures of toxic substances. Knowing the effects of contaminants as a mixture compared to their effects in isolated form is therefore important. This study aimed to evaluate the oxidative stress induced by binary mixtures of diclofenac with paracetamol, ibuprofen, naproxen, and acetylsalicylic acid and by these nonsteroidal anti-inflammatory drugs (NSAIDs) in isolated form, using Hyalella azteca as a bioindicator. The median lethal concentration (LC50) and the lowest observed adverse effect level (LOAEL) of each NSAID were obtained. Amphipods were exposed for 72 h to the latter value in isolated form and as binary mixtures. The following biomarkers were evaluated: lipid peroxidation (LPX), protein carbonyl content (PCC), and activity of the antioxidant enzymes: superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GPx). Significant increases in LPX and PCC with respect to the control group (p ≤ 0.05) were induced by NSAIDs both in isolated form and as binary mixtures. Changes in SOD, CAT, and GPx activity likewise occurred with NSAIDs in isolated form and as binary mixtures. In conclusion, NSAIDs used in this study induce oxidative stress on H. azteca both in isolated form and as binary mixtures, and the interactions occurring between these pharmaceuticals are probably antagonistic in type.

  8. Acetylsalicylic acid-induced oxidative stress, cell cycle arrest, apoptosis and mitochondrial dysfunction in human hepatoma HepG2 cells.

    Science.gov (United States)

    Raza, Haider; John, Annie; Benedict, Sheela

    2011-10-01

    It is widely accepted that non-steroidal anti-inflammatory drugs (NSAIDs), including aspirin, reduce the risk of cancer. The anti-cancer and anti-inflammatory effects of NSAIDs are associated with the inhibition of prostaglandin synthesis and cyclooxygenase-2 activity. Several other mechanisms which contribute to the anti-cancer effect of these drugs in different cancer models both in vivo and in vitro are also presumed to be involved. The precise molecular mechanism, however, is still not clear. We investigated, therefore, the effects of acetylsalicylic acid (ASA, aspirin) on multiple cellular and functional targets, including mitochondrial bioenergetics, using human hepatoma HepG2 cancer cells in culture. Our results demonstrate that ASA induced G0/G1 cell cycle arrest and apoptosis in HepG2 cells. ASA increased the production of reactive oxygen species, reduced the cellular glutathione (GSH) pool and inhibited the activities of the mitochondrial respiratory enzyme complexes, NADH-ubiquinone oxidoreductase (complex I), cytochrome c oxidase (complex IV) and the mitochondrial matrix enzyme, aconitase. Apoptosis was triggered by alteration in mitochondrial permeability transition, inhibition of ATP synthesis, decreased expression of the anti-apoptotic protein Bcl-2, release of cytochrome c and activation of pro-apoptotic caspase-3 and the DNA repairing enzyme, poly (-ADP-ribose) polymerase (PARP). These findings strongly suggest that ASA-induced toxicity in human hepatoma HepG2 cells is mediated by increased metabolic and oxidative stress, accompanied by mitochondrial dysfunction which result in apoptosis.

  9. Histopathological, Ultrastructural, and Immunohistochemical Assessment of Hippocampus Structures of Rats Exposed to TCDD and High Doses of Tocopherol and Acetylsalicylic Acid

    Directory of Open Access Journals (Sweden)

    Joanna Rosińczuk

    2015-01-01

    Full Text Available The effect of 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD on central nervous system consists of changing expression of estrogen receptors, whereas the result of chronic inflammatory reaction caused by dioxin is occurrence of destructive changes in various organs connected with disturbed metabolism of connective tissue and damage of cells. The aim of the study was to determine the effect of dioxins on function, ultrastructure, and cytological and histological structure of hippocampus, particularly on expression of estrogen receptors in central nervous system as well as to define protective influence of tocopherol (TCP and acetylsalicylic acid (ASA on the decrease in activity of proinflammatory effects in central nervous system. It was shown that TCDD contributes to destructive and inflammatory changes along with demyelization of myelin sheaths and atrophy of estrogen receptors in hippocampus. Dioxin contributes to atrophy of estrogen receptors in hippocampus, in which also destructive and inflammatory changes were found along with demyelination of myelin sheaths. Histopathological and ultrastructural image of hippocampus areas in rats, in which both TCP and ASA were used, is characterized by poorly expressed degenerative changes and smaller inflammatory reactivity. Using both TCP and ASA has a protective effect on functions of central nervous system.

  10. Evaluation of platelet function using PFA-100® in patients treated with Acetylsalicylic acid and qualified for Trauma and Orthopedic surgery procedures.

    Science.gov (United States)

    Kurak, J; Zając, P; Czyżewski, D; Kucharski, R; Grzanka, R; Kasperska-Zajac, A; Koczy, B

    2016-11-01

    The phenomenon of high on-acetylsalicylic acid (ASA) treatment platelet (PLT) reactivity - HATPR - and its clinical implications have not been fully understood. Little data is available on assessing PLT activity based on the severity of intra- and postoperative bleeding in a population of orthopedic patients with normal closure time (CT) measured by a PLT function analyzer PFA-100®, despite being given long-term ASA therapy. The aim is to assess PLT function using PFA-100® in patients with ASA therapy and qualified for trauma and orthopedic surgery procedures. The retrospective analysis covered 384 patients whose PLT reactivity was assessed using PFA-100®. Out of those, 198 had been taking ASA with a 75 mg dose until hospital admission. In addition, a group of 70 patients with a proximal femoral fracture surgically treated using the dynamic hip screw (DHS) was selected, in whom severity of bleeding was assessed by HIP ASA (+). The reference group comprised 52 patients (without ASA therapy) who were operated on due to the same indications. Normal CT was found in 37% of ASA-receiving patients. Patients with normal CT, despite ASA therapy, exhibited significantly more intense bleeding after DHS surgery. A similar number of patients required red blood cells (RBCs) transfusion in HIP ASA (+) and HIP ASA (-). Increased risk of complications in HIP ASA (+) group was not found.

  11. Protective Role of Acetylsalicylic Acid in Experimental Trypanosoma cruzi Infection: Evidence of a 15-epi-Lipoxin A4-Mediated Effect

    Science.gov (United States)

    Henriquez, Natalia; Faúndez, Mario; Torres, Gloria; Castillo, Christian; Escanilla, Sebastián; Kemmerling, Ulrike; Morello, Antonio; López-Muñoz, Rodrigo A.; Maya, Juan D.

    2013-01-01

    Chagas' disease, produced by Trypanosoma cruzi, affects more than 8 million people, producing approximately 10,000 deaths each year in Latin America. Migration of people from endemic regions to developed countries has expanded the risk of infection, transforming this disease into a globally emerging problem. PGE2 and other eicosanoids contribute to cardiac functional deficits after infection with T. cruzi. Thus, the inhibition of host cyclooxygenase (COX) enzyme emerges as a potential therapeutic target. In vivo studies about the effect of acetylsalicylic acid (ASA) upon T. cruzi infection are controversial, and always report the effect of ASA at a single dose. Therefore, we aimed to analyze the effect of ASA at different doses in an in vivo model of infection and correlate it with the production of arachidonic acid metabolites. ASA decreased mortality, parasitemia, and heart damage in T. cruzi (Dm28c) infected mice, at the low doses of 25 and 50 mg/Kg. However, this effect disappeared when the high ASA doses of 75 and 100 mg/Kg were used. We explored whether this observation was related to the metabolic shift toward the production of 5-lipoxygenase derivatives, and although we did not observe an increase in LTB4 production in infected RAW cells and mice infected, we did find an increase in 15-epi-LXA4 (an ASA-triggered lipoxin). We also found high levels of 15-epi-LXA4 in T. cruzi infected mice treated with the low doses of ASA, while the high ASA doses decreased 15-epi-LXA4 levels. Importantly, 15-epi-LXA4 prevented parasitemia, mortality, and cardiac changes in vivo and restored the protective role in the treatment with a high dose of ASA. This is the first report showing the production of ASA-triggered lipoxins in T. cruzi infected mice, which demonstrates the role of this lipid as an anti-inflammatory molecule in the acute phase of the disease. PMID:23638194

  12. COMPARISON OF ANTIPLATELET EFFICACY OF ORIGINAL AND GENERIC ENTEROSOLUBLE ACETYLSALICYLIC ACID IN PATIENTS WITH HIGH CARDIOVASCULAR RISK. SIMPLE BLIND CROSSED RANDOMIZED CONTROLLED STUDY (IKAR

    Directory of Open Access Journals (Sweden)

    S. Yu. Martsevich

    2010-01-01

    Full Text Available Aim. To compare the antiplatelet efficacy of the original and generic enterosoluble tableted acetylsalicylic acid (ASA in patients with high cardiovascular risk.Material and мethods. Patients (n=30 with high cardiovascular risk and indications for the ASA therapy were included in the study. Antiplatelet agents were withdrawn 3 weeks before study start (wash-out period. Study drugs were distributed at the start visit according to the randomization scheme. The first study drug course was 3 weeks, then next wash-out period lasting 3 weeks, and at last the second study drug course during 3 weeks occurred. Blood samples were taken; blood pressure and heart rate were recorded before and after therapies. ASA antiplatelet effect was evaluated by spontaneous and ADP-induced platelet aggregation assessment. Platelet aggregation was determined by the change turbidimetric translucent ability of the blood sample during the formation of aggregates after 2 minutes of exposure. ADP solution of three concentrations (0.5, 1 and 2 µMol was used as an inductor of aggregation.Results. Significant differences between the compared drugs in effect on platelet aggregation, blood pressure and heart rate were not found. Signs of platelet desaggregation after 3 weeks of generic ASA therapy were found in 65, 34.5 and 31% of patients when aggregation was tested with ADP 0.5, 1 and 2 µMol respectively. Desaggregation was revealed in 65.4, 42.3 and 31% of patients treated with original ASA (p>0.05 in the same test and the same ADP inducing concentration.. Adverse events associated with study drugs were not registered.Conclusion. ASA generic Trombopol ® 75 mg (Pharmaceutical Factory Polpharma SA, Poland and ASA original Aspirin® Cardio (Bayer AG, Germany are equivalent in antiplatelet effect and tolerability.

  13. The effect of different doses and different routes of acetylsalicylic acid administration on platelet aggregation in healthy volunteers and ischemic stroke patients.

    Science.gov (United States)

    Chýlová, Miroslava; Moťovská, Zuzana; Osmančík, Pavel; Procházka, Bohumír; Kalvach, Pavel

    2015-04-01

    The purpose was to assess the effect of different doses and different routes of acetylsalicylic acid (ASA) administration on platelet aggregation and the comparison between platelet aggregation after the single and the repetitive administration of ASA in healthy individuals and in patients after ischemic stroke. The study group consists of 22 healthy individuals and 30 patients with documented ischemic stroke. Platelet aggregation was measured in healthy individuals: (a) twice before ASA and (b) 2 h after different single doses and different routes of ASA administration-(b1) 500 mg orally, (b2) 500 mg intravenously, and (b3) 100 mg orally. We measured aggregability in healthy individuals after five consecutive days of 100 mg of ASA q.d. and in patients on chronic ASA 100 mg q.d. The VerifyNow was used with results expressed in aspirin reaction units (ARU). In healthy individuals, the dose-(b1) 500 mg orally-reduced the aggregability to mean (SD) 392 (36) ARU (p administration, and the same is true for the suppression after single dose of 500 mg orally and 100 mg orally (p = 0.011). Oral dose 100 mg for 5 days in healthy individuals reduced aggregation to 405 (37) and in post-stroke patients to 433 (54). All doses of ASA, both orally and intravenously, have produced a significant reduction of platelet aggregation. Preference of the parenteral to oral application has not been established.

  14. Adjuvant effect of caffeine on acetylsalicylic acid anti-nociception: prostaglandin E2 synthesis determination in carrageenan-induced peripheral inflammation in rat.

    Science.gov (United States)

    Fernández-Dueñas, Víctor; Sánchez, Sílvia; Planas, Eulàlia; Poveda, Raquel

    2008-02-01

    In the present study, we report a synergistic interaction between acetylsalicylic acid (ASA) and caffeine (CAF) on the inhibition of nociception in a model of peripheral inflammation in rat; on the contrary no interaction have been found on anti-inflammatory effects and peripheral prostaglandin E2 (PGE-2) synthesis inhibition. Acute inflammation was induced by the subplantar injection of carrageenan into the right hind paw, and the effects of the drugs were evaluated from 0 to 5h. Nociception was assessed using the Randall & Selitto test, and the inflammatory response by plethismometry. Oral administration of ASA (10-400mg/kg) induced dose-related anti-nociceptive and anti-inflammatory effects. On the other hand, oral CAF administration (5-50mg/kg) did not show a dose-related inhibitory effect, neither on the inhibition of nociception nor on the inflammatory response. To analyze a possible interaction between both drugs a dose-response curve to ASA plus a fixed dose of CAF (5mg/kg) was obtained 3h after the injection of carrageenan, when the inflammatory pain peaked. A fixed dose of CAF was able to improve the anti-nociceptive, but not the anti-inflammatory, effects of ASA. We also assessed, by enzyme immunoassay, the effects of the combination on peripheral PGE-2 levels: CAF did not alter the inhibitory effect of ASA on PGE-2 synthesis. Our results corroborate the well-known clinical effects of combining ASA and CAF; on the other hand, we rule out that prostaglandin synthesis inhibition at peripheral sites would be the mechanism responsible of the adjuvant anti-nociceptive effect of CAF.

  15. Acetylsalicylic acid regulates overexpressed small GTPase RhoA in vascular smooth muscle cells through prevention of new synthesis and enhancement of protein degradation.

    Science.gov (United States)

    Li, Dong-Bo; Fu, Zhi-Xuan; Ruan, Shu-Qin; Hu, Shen-Jiang; Li, Xia

    2012-04-01

    RhoA has been shown to play a major role in vascular processes and acetylsalicylic acid (aspirin) is known to exert a cytoprotective effect via multiple mechanisms. In the present study, we aimed at investigating the effect of aspirin on RhoA expression under a stress state in rat VSMCs (vascular smooth muscle cells) and the underlying mechanisms. The expression of iNOS (inducible nitric oxide synthase) and iNOS activity as well as NO concentration was significantly promoted by LPS (lipopolysaccharide) accompanying the elevation of RhoA expression, which was blocked by the addition of the iNOS inhibitor L-NIL [L-N6-(1-iminoethyl)lysine dihydrochloride]. Aspirin (30 μM) significantly attenuated the elevation of RhoA, while indomethacin and salicylate had no similar effect. The sGC (soluble guanylate cyclase) inhibitor ODQ (1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one) showed the same effect as aspirin in down-regulating RhoA but was reversed by the addition of the cGMP analogue 8-Br-PET-cGMP (β-phenyl-1,N2-ethano-8-bromoguanosine 3',5'-cyclic monophosphorothioate). 8-Br-PET-cGMP solely enhanced the RhoA expression that was abrogated by preincubation with aspirin. Degradation analysis indicated that aspirin enhanced the protein degradation rate of RhoA and GDP-bound RhoA seemed to be more susceptible to aspirin-enhanced degradation compared with the GTP-bound form. Our results indicate that aspirin attenuates the LPS-induced overexpression of RhoA both by inhibiting new synthesis and accelerating protein degradation, which may help elucidate the multiple beneficial effects of aspirin.

  16. Reduced mucosal side-effects of acetylsalicylic acid after conjugation with tris-hydroxymethyl-aminomethane. Synthesis and biological evaluation of a new anti-inflammatory compound.

    Science.gov (United States)

    Varga, Gabriella; Lajkó, Norbert; Ugocsai, Melinda; Érces, Dániel; Horváth, Gyöngyi; Tóth, Gábor; Boros, Mihály; Ghyczy, Miklós

    2016-06-15

    Acetylsalicylic acid (ASA) causes adverse haemorrhagic reactions in the upper gastrointestinal (GI) tract, and previous results have suggested that combination therapy with 2-amino-2-(hydroxymethyl)-1,3-propanediol (Tris) could provide protection in this scenario. Based on this hypothesis, our aim was to develop a new compound from ASA and Tris precursors and to characterize the biological effects of ASA-Tris and the derivatives ASA-bis- and mono-hydroxymethyl-aminomethane (ASA-Bis, ASA-Mono, respectively) using in vivo and in vitro test systems. ASA or ASA conjugates (0.55mmol/kg, each) were administered intragastrically to Sprague-Dawley rats. Changes in the mucosal structure and in the serosal microcirculation were detected by in vivo imaging techniques, the plasma TNF-alpha, tissue xanthine oxidoreductase and myeloperoxidase activities, and liver cytochrome c changes were also determined. In two separate series, platelet aggregation and carrageenan arthritis-induced inflammatory pain were measured in control, ASA and ASA-Tris-treated groups. Severe mucosal injury and a significant decrease in serosal red blood cell velocity developed in the ASA-treated group and an ~2-fold elevation in proinflammatory mediator levels evolved. ASA-Tris did not cause bleeding, microcirculatory dysfunction, mucosal injury or an elevation in proinflammatory markers. The ASA-Mono and ASA-Bis conjugates did not cause macroscopic bleeding, but the inflammatory activation was apparent. ASA-Tris did not influence the cyclooxygenase-induced platelet aggregation significantly, but the inflammatory pain was reduced as effectively as in the case of equimolar ASA doses. ASA-Tris conjugation is an effective approach through which the GI side-effects of ASA are controlled by decreasing the cytokine-mediated progression of pro-inflammatory events.

  17. The Teaching Reform and Exploration on Synthesis Experiments of Acetylsalicylic Acid%乙酰水杨酸合成实验教学改革与探索

    Institute of Scientific and Technical Information of China (English)

    耿会玲; 逯嫒琳; 于新池; 袁茂森; 王俊儒

    2016-01-01

    文章通过对比国内外大学教材中乙酰水杨酸合成实验,在前人基础上推陈出新,兼顾实验技能系统训练和内容探索研究,对经典实验内容和方法进行改革与创新,建立了开放创新型实验体系.实践表明,创新性教学内容的引入和教学方法的改革激发了学生的求知欲,使学生在知识和技能的获取中变被动为主动,既提高了实验操作技能,又提升了创新思维能力和团队协作能力,为后续专业学习和科学研究奠定了坚实基础,达到了预期的教学效果.%Through comparing the synthesis experiments of acetylsalicylic acid in domestic and foreign textbooks,based on previous fundamental and seminal study,the paper explores the system training of exper-imental skills and content, reforms and innovates the traditional experimental contents and method, and builds open innovative experiment system. The practice shows that the introduction of innovative teaching con-tent and the reform of teaching method can stimulate studentsˊdesire to acquire knowledge,change their atti-tude to further obtain knowledge and skills from passivity to activation,enhance their experimental operation skills,improve their innovative thinking ability and team cooperation ability,lay the firm foundation for future professional learning and scientific research,and achieve expected teaching results.

  18. A comparative study between conventional pan coater and quasi-continuous small batch coater on the stability of tablets containing acetylsalicylic acid.

    Science.gov (United States)

    Cahyadi, Christine; Chan, Lai Wah; Heng, Paul Wan Sia

    2015-02-01

    The Supercell coater was developed as an in-line small batch tablet coater which uses air-fluidization for tablet coating. Coating time is very much reduced, with improved heat and mass transfer. It was hypothesized that the quasi-continuous Supercell coating process was more suitable for the aqueous coating of tablets containing moisture-sensitive drugs. Acetylsalicylic acid (ASA) was used as the model drug in this study. The extent of ASA degradation in Supercell coating was compared against that of tablets coated using the conventional pan coater. Less than 0.3% of ASA was degraded at the end of the coating process using either coater. The extent of ASA degradation was found to be more pronounced during storage. The Supercell coated tablets exhibited comparable or smaller percentage of ASA degradation than the pan coated tablets at the end of a storage period of 6 months under accelerated stability conditions (40°C/75% RH) and 3 years under ambient conditions (25°C/50% RH). The extent and rate of ASA degradation during storage were dependent on the processing conditions employed during Supercell coating. Increase in temperature generally led to a reduction in ASA degradation, while increase in spray rate and coating level caused more degradation. Greater extent of ASA degradation was observed on the surface of pan coated tablets compared with Supercell coated tablets due to greater moisture contact and the slower and wetter coating process. Changes to the processing conditions also influenced the residual moisture content (0.55-2.86%) of the tablets. However, no direct correlation between the residual moisture content of the tablets after coating and the extent of ASA degradation during storage was found.

  19. The Effect of Roux-en-Y Gastric Bypass Surgery in Morbidly Obese Patients on Pharmacokinetics of (Acetyl)Salicylic Acid and Omeprazole: the ERY-PAO Study

    NARCIS (Netherlands)

    Mitrov-Winkelmolen, Lieke; van Buul-Gast, Marie Christine W; Swank, Dingeman J.; Overdiek, Hans W P M; van Schaik, Ron H N; Touw, Daan J.

    2016-01-01

    Background Data on the absorption of orally administered drugs following Roux-en-Y gastric bypass (RYGB) surgery in obese patients are limited and inconclusive. As it is difficult to predict changes in absorption, studies on frequently used drugs in this population are necessary. Acetylsalicylic aci

  20. 联合应用双嘧达莫和阿司匹林在卒中二级预防中的疗效评价%Evaluation of Dipyridamole and Acetylsalicylic Acid in the Secondary Prevention of Stroke

    Institute of Scientific and Technical Information of China (English)

    张雄; 王丽娟

    2005-01-01

    @@ 1文献类型 预防. 2证据水平 1b. 3文献来源 ①Diener HC, Cunha L, Forbes C, et al.European Stroke Prevention Study 2. Dipyridamole and Acetylsalicylic acid in the secondary prevention of stroke [J]. J Neurol Sci, 1996, 143(1-2):1-13.②Sacco RL, Sivenius J, Diener HC. Efficacy of Aspirin plus extended-release Dipyridamole in preventing recurrent stroke in high-risk populations [J]. Arch Neurol, 2005,62(3):403-408.

  1. EDCI/DMAP存在下7-乙基喜树碱与乙酰水杨酸的反应%Studies on esterification reaction of 7-ethylcamptothecin and acetylsalicylic acid in presence of EDCI/DMAP

    Institute of Scientific and Technical Information of China (English)

    蔡冉; 王浦海; 孙立; 袁胜涛

    2016-01-01

    以EDCI为脱水剂,DMAP为催化剂,对7-乙基喜树碱与乙酰水杨酸的酯化反应进行了研究。经硅胶柱层析纯化和波谱结构鉴定,所得产物并非预期的酯化产物———20(S)-O-乙酰水杨酸-7-乙基喜树碱酯(2),而是20(S)-O-乙酸-7-乙基喜树碱酯(3)。推测在此条件下7-乙基喜树碱优先与乙酰水杨酸的酯基之间发生了酯交换反应,通过反应机理对上述反应结果进行了解释。化合物3在8 mg·kg-1剂量腹腔给药,对小鼠肉瘤S180较弱抑瘤活性。%The esterification reaction of acetylsalicylic acid and 7-ethylcamptothecin in presence of EDCI/DMAP was investigated. The product was purified by silica gel column chromatography and the structure was identified by IR,1 HNMR and HR-MS. The product was not expected 7-ethylcamptothecin acetylsalicylate(2)but 7-ethylcamptothecin acetate(3). It was speculated that ester exchange reaction between hydroxy group of 7-ethylcamptothecin and ester group of acetylsalicylic acid was preferentially occurred under the reaction condition. The reaction result might be explained by an ester exchange reaction mechanism. Compound 3(i. p. 8 mg·kg-1 ) had weak antitumor effect on S180 mice model.

  2. Bleeding peptic ulcer. Prevalence of Helicobacter pylori and use of nonsteroidal anti-inflammatory drugs/acetylsalicylic acid

    DEFF Research Database (Denmark)

    Vestergard, A.; Bredahl, K.; Muckadell, O.B. de

    2009-01-01

    INTRODUCTION: Helicobacter pylori (HP) infection and use of nonsteroidal anti-inflammatory drugs (NSAIDs)/acetyl salicylic acid (ASA) are risk factors for bleeding peptic ulcer. HP eradication reduces the risk of rebleeding. Antibiotics, proton pump inhibitors (PPI) and presence of blood in the s......INTRODUCTION: Helicobacter pylori (HP) infection and use of nonsteroidal anti-inflammatory drugs (NSAIDs)/acetyl salicylic acid (ASA) are risk factors for bleeding peptic ulcer. HP eradication reduces the risk of rebleeding. Antibiotics, proton pump inhibitors (PPI) and presence of blood...

  3. Homocysteine is a novel risk factor for suboptimal response of blood platelets to acetylsalicylic acid in coronary artery disease: a randomized multicenter study.

    Science.gov (United States)

    Karolczak, Kamil; Kamysz, Wojciech; Karafova, Anna; Drzewoski, Jozef; Watala, Cezary

    2013-08-01

    The incomplete inhibition of platelet function by acetylsalicylic acid (ASA), despite the patients are receiving therapeutic doses of the drug ('aspirin-resistance'), is caused by numbers of risk factors. In this study we verified the idea that plasma homocysteine (Hcy) contributes to 'aspirin-resistance' in patients with coronary artery disease (CAD) and with or without type 2 diabetes mellitus (T2DM). A cross-designed randomized controlled intervention study has been performed (126 CAD pts incl. 26 with T2DM) to determine whether increasing ASA dose from 75mg to 150mg daily may result in the increased antiplatelet effect, in the course of four-week treatment. Platelet response to collagen (coll) or arachidonic acid (AA) was monitored with whole blood aggregometry, plasma thromboxane (Tx), and Hcy levels were determined immunochemically. The ASA-mediated reductions in platelet response to coll (by 12±3%) or AA (by 10±3%) and in plasma Tx (by 20±9%; p<0.02 or less) were significantly greater for higher ASA dose and significantly correlated with plasma Hcy, which was significantly lower in "good" ASA responders compared to "poor" responders (p<0.001). Higher plasma Hcy appeared a significant risk factor for blood platelet refractoriness to low ASA dose (OR=1.11; ±95%CI: 1.02-1.20, p<0.02, adjusted to age, sex and CAD risk factors). Hcy diminished in vitro antiplatelet effect of low ASA concentration and augmented platelet aggregation (by up to 62% (p<0.005) for coll and up to 15% (p<0.005) for AA), whereas its acetyl derivative acted oppositely. Otherwise, Hcy intensified antiplatelet action of high ASA. Hyperhomocysteinaemia may be a novel risk factor for the suppressed blood platelet response to ASA, and homocysteine may act as a specific sensitizer of blood platelets to some agonists. While homocysteine per se acts as a proaggregatory agent to blood platelets, its acetylated form is able to reverse this effect. Thus, these findings reveal a possibly new

  4. Role of the double-contrast barium enema in rectal stenosis due to suppositories containing paracetamol and acetylsalicylic acid

    Energy Technology Data Exchange (ETDEWEB)

    Tannouri, F.; Lalmand, B.; Zalcman, M.; Gansbeke, D. van; Gevenois, P.A.; Struyven, J. [Department of Radiology, Hopital Erasme, University of Brussels (Belgium); Peny, M.O. [Department of Pathology, University of Brussels (Belgium); Gossum, A. van [Department of Gastroenterology, University of Brussels (Belgium)

    1998-09-01

    Self-treatment of chronic headache with suppositories containing paracetamol and acetylsalaicylic acid may lead to serious complications. We report the radiological features of five cases of rectal stenosis following the use of such suppositories. The role of the double-contrast barium enema in suggesting the diagnosis of this complication of a chronic and often unrecognized self-treatment is emphasized. (orig.) With 6 figs., 20 refs.

  5. Determination of acetylsalicylic acid and its major metabolite, salicylic acid, in human plasma using liquid chromatography-tandem mass spectrometry: application to pharmacokinetic study of Astrix in Korean healthy volunteers.

    Science.gov (United States)

    Bae, Soo Kyung; Seo, Kyung Ah; Jung, Eun Ji; Kim, Ho-Sook; Yeo, Chang-Woo; Shon, Ji-Hong; Park, Kyung-Mi; Liu, Kwang-Hyeon; Shin, Jae-Gook

    2008-06-01

    The first liquid chromatography-tandem mass spectrometry (LC/MS/MS) method for determination of acetylsalicylic acid (aspirin, ASA) and one of its major metabolites, salicylic acid (SA), in human plasma using simvastatin as an internal standard has been developed and validated. For ASA analysis, a plasma sample containing potassium fluoride was extracted using a mixture of ethyl acetate and diethyl ether in the presence of 0.5% formic acid. SA, a major metabolite of ASA, was extracted from plasma using protein precipitation with acetonitrile. The compounds were separated on a reversed-phase column with an isocratic mobile phase consisting of acetonitrile and water containing 0.1% formic acid (8:2, v/v). The ion transitions recorded in multiple reaction monitoring mode were m/z 179 --> 137, 137 --> 93 and 435 --> 319 for ASA, SA and IS, respectively. The coefficient of variation of the assay precision was less than 9.3%, and the accuracy exceeded 86.5%. The lower limits of quantification for ASA and SA were 5 and 50 ng/mL, respectively. The developed assay method was successfully applied for the evaluation of pharmacokinetics of ASA and SA after single oral administration of Astrix (entero-coated pellet, 100 mg of aspirin) to 10 Korean healthy male volunteers.

  6. 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.

  7. Exantema hemorrágico por virus dengue inducido por ácido acetil-salicílico Haemorrhagic exanthema due to dengue virus induced by acetylsalicylic acid

    Directory of Open Access Journals (Sweden)

    L. Valerio

    2006-12-01

    Full Text Available El dengue, enfermedad infecciosa vírica propia de los climas tropicales, se considera una patología reemergente que ha dado lugar a graves epidemias en la última década. En la expansión del virus y de su mosquito vector se barajan factores relacionados con la alteración humana del medio, con la rapidez en el tránsito de mercancias y personas y debidos al cambio climático. Como reflejo de ello, se asiste a un aumento de casos importados que, al ser una enfermedad con periodo de incubación corto (7-10 días, afecta especialmente a turistas procedentes de áreas endémicas. El reconocimiento de los antecedentes personales de viajes, de los síntomas-guía de la enfermedad y de las potenciales complicaciones (dengue hemorrágico deben ser incluidos en una anamnesis para el estudio de fiebre de origen desconocido o de exantema febril. Se presenta el caso de una paciente cuya clínica de dengue clásico se agravó por el autotratamiento con ácido acetil-salicílico.Dengue fever, a viral infectious disease characteristic of tropical climates, is considered to be a re-emergent pathology responsible for several serious outbreaks in the last decade. Some factors have been involved in the spread of the virus and its vectorial mosquito carrier: human alteration of the ecosystems, improvement and speed in the transit of goods and people and climate changes. As a reflection of this, an increase in imported cases is probable, especially in tourists coming from endemic areas, considering its short period of incubation (7-10 days. The recognition of personal antecedents of journeys, the main symptoms of the disease and the potential presence of complications (haemorrhagic dengue should be included in the examination of fever of unknown origin or feverish exanthema. The case of a patient is presented whose clinical picture of classic dengue fever was worsened by self-treatment with acetylsalicylic acid.

  8. Semi-physiologic model validation and bioequivalence trials simulation to select the best analyte for acetylsalicylic acid.

    Science.gov (United States)

    Cuesta-Gragera, Ana; Navarro-Fontestad, Carmen; Mangas-Sanjuan, Victor; González-Álvarez, Isabel; García-Arieta, Alfredo; Trocóniz, Iñaki F; Casabó, Vicente G; Bermejo, Marival

    2015-07-10

    The objective of this paper is to apply a previously developed semi-physiologic pharmacokinetic model implemented in NONMEM to simulate bioequivalence trials (BE) of acetyl salicylic acid (ASA) in order to validate the model performance against ASA human experimental data. ASA is a drug with first-pass hepatic and intestinal metabolism following Michaelis-Menten kinetics that leads to the formation of two main metabolites in two generations (first and second generation metabolites). The first aim was to adapt the semi-physiological model for ASA in NOMMEN using ASA pharmacokinetic parameters from literature, showing its sequential metabolism. The second aim was to validate this model by comparing the results obtained in NONMEM simulations with published experimental data at a dose of 1000 mg. The validated model was used to simulate bioequivalence trials at 3 dose schemes (100, 1000 and 3000 mg) and with 6 test formulations with decreasing in vivo dissolution rate constants versus the reference formulation (kD 8-0.25 h (-1)). Finally, the third aim was to determine which analyte (parent drug, first generation or second generation metabolite) was more sensitive to changes in formulation performance. The validation results showed that the concentration-time curves obtained with the simulations reproduced closely the published experimental data, confirming model performance. The parent drug (ASA) was the analyte that showed to be more sensitive to the decrease in pharmaceutical quality, with the highest decrease in Cmax and AUC ratio between test and reference formulations.

  9. Prospective, randomised trial of the time dependent antiplatelet effects of 500 mg and 250 mg acetylsalicylic acid i. v. and 300 mg p. o. in ACS (ACUTE).

    Science.gov (United States)

    Zeymer, Uwe; Hohlfeld, Thomas; Vom Dahl, Jürgen; Erbel, Raimund; Münzel, Thomas; Zahn, Ralf; Roitenberg, Alexander; Breitenstein, Stefanie; Pap, Ákos Ferenc; Trenk, Dietmar

    2017-02-28

    Little is known about the onset of action after intravenous or oral administration of acetylsalicylic acid (ASA) in patients with acute coronary syndromes (ACS). The aim of the study was to compare intravenous 250 or 500 mg acetylsalicylic acid (ASA) with oral 300 mg in ASA naïve patients with ACS concerning the onset of antiplatelet effects measured by time dependent thromboxane inhibition. A total of 270 patients with ACS acid (AA)-induced platelet thromboxane release (TXB2) 5 minutes (min) after study drug administration. Both 250 mg and 500 mg ASA i. v. inhibited TXB2 formation nearly completely (geometric means: from 581.7 and 573.9 ng/ml at baseline to 3.9 and 3.1 ng/ml at 5 min, respectively) compared to 300 mg oral ASA (geometric means: from 652.0 to 223.7 ng/ml) (p-value, ANCOVA: < 0.0001). Similar results were obtained for inhibition of AA-induced platelet aggregation (Multiplate ASPItest; from means 86.41 and 85.72 U to 23.04 and 20.57 U at 5 min, respectively) compared to 300 mg oral ASA from mean 87.18 to 75.56 U (p-value, ANCOVA: <0.0001). The rate of bleedings was low and comparable between the groups. In summary, the administration of a single dose of 250 or 500 mg ASA IV compared to 300 mg orally is associated with a faster and more complete inhibition of thromboxane generation and platelet aggregation. Bleeding complications were comparable between the groups.

  10. The effect of salicylic acid and acetylsalicylic acid on red pigment formation in mechanically wounded scales of Hippeastrum x hybr. hort. and on the growth and development of Phoma narcissi

    Directory of Open Access Journals (Sweden)

    Alicja Saniewska

    2012-12-01

    Full Text Available Various organs of Hippeastrum infected by Phoma narcissi, infested with mite, Steneotarsonemus laticeps or mechanically wounded, produce red pigment on the surface of injured tissues. The aim of the present work was to study the effect of salicylic (SA and acetylsalicylic acids (ASA (inhibitors of biosynthesis of jasmonates and ethylene on red pigment formation in wounded scales of bulbs of Hippeastrum and on the mycelium growth of P. narcissi in vivo and in vitro. SA and ASA at a concentration of 1 and 2 mM partially inhibited the formation of red pigment in wounded scales, first of all in first 2 days after treatment. The growth and development of P. narcissi on basal plate and scales of longitudinally cut Hippeastrum bulb treated with SA and ASA (1 and 2 mM was similar as in control. SA (50 µg·cm-3 and ASA (250 µg·cm-3 inhibited the mycelium growth of P. narcissi on PDA medium, and concentration of 1000 µg·cm-3 of both almost totally inhibited the mycelium growth of the pathogen. Inhibitory effect of SA and ASA on the formation of red pigment in wounded scales of Hippeastrum may be caused by lowered biosynthesis and accumulation of jasmonates.

  11. Quantitative Analysis of Active Ingredients in Compound Acetylsalicylic Acid Tablets by DOSY%复方乙酰水杨酸片中有效成分的DOSY技术分析

    Institute of Scientific and Technical Information of China (English)

    王丽敏; 仇汝臣; 黄少华

    2016-01-01

    Compound acetylsalicylic acid tablet is a clinical drug having antipyretic, analgesic and anti-inflammatory effects. The present methods to analyze the active ingredients in this drug have many disadvantages. In this study, we used polydimethylsiloxane (PDMS)-assisted diffusion ordered NMR spectroscopy (DOSY), DOSY-correlated spectroscopy (COSY), and relative quantitative1H NMR techniques to analyze the three main active ingredients in this drug. The content ratios among the 3 components could be obtained. It is argued that PDMS-assisted DOSY provides a convenient and efficient method for pharmaceutical quality control of compound acetylsalicylic acid tablets.%复方乙酰水杨酸片是临床常用的解热镇痛消炎药物,目前其有效成分的分析方法存在操作繁琐而分析速度慢等不足。该文利用二甲基硅油(PDMS)辅助的扩散排序(DOSY)技术以及扩散排序-同核相关(DOSY-COSY)联用技术,成功地对复方乙酰水杨酸片中三种有效成分的分子结构进行了快速定性分析,并且利用核磁共振氢谱(1H NMR)技术进行了相对定量分析。该方法具有方便、快捷等特点,可作为借鉴和参考用于药物的质量评价。

  12. 凹凸棒黏土负载型固体酸催化合成乙酰水杨酸%Synthesis of Acetylsalicylic Acid over Attapulgite Supported Solid Acid Catalyst

    Institute of Scientific and Technical Information of China (English)

    吴洁; 蒋金龙; 钱晓敏

    2011-01-01

    Attapulgite (ATP) supported H+ and AlCl3 solid acid catalysts (H+/ATP and AlCl3/ATP) were prepared and their catalytic activities for synthesis of acetylsalicylic acid (AA) from salicylic acid and acetic anhydride were compared with the free acids.The results suggested that the solid acid catalysts exhibited higher activity than those of the free acids, especially AlCl3/ATP catalyst.Under the optimum conditions of AlCl3/ATP catalyst mass fraction 5% (based on salicylic acid), reaction temperature 80 ℃, reaction time 30 min and mole ratio of acetic anhydride to salicylic acid 2.0, the yield and the purity of AA reached 92.5% and 99.5% respectively.The synthesized AA was characterized by means of FTIR and 1H NMR.The AA yield still reached 89.2% after it was regenerated and reused for 5 times.%以凹凸棒黏土(ATP)为载体,制备了负载H+和AlCl3的固体酸催化剂(分别标记为H+/ATP,AlCl3/ATP),比较了负载前后催化剂对乙酰水杨酸合成反应的催化活性.实验结果表明,固体酸催化剂的活性高于游离酸催化剂,其中AlCl3/ATP催化剂的活性最高.以AlCl3/ATP为催化剂催化合成乙酰水杨酸的最佳工艺条件为:催化剂用量为5%(基于水杨酸质量),n(乙酸酐):n(水杨酸)=2.0,反应温度80℃,反应时间30 min;在此条件下,乙酰水杨酸收率达92.5%,纯度为99.5%.用FTIR和1H NMR表征了产物结构.AlCl3/ATP催化剂经活化再生重复使用5次后,乙酰水杨酸收率仍可达89.2%,表明AlCl3/ATP催化剂具有一定的稳定性,可实现再生利用.

  13. Simultaneous extraction of acetylsalicylic acid and salicylic acid from human plasma and simultaneous estimation by liquid chromatography and atmospheric pressure chemical ionization/tandem mass spectrometry detection. Application to a pharmacokinetic study.

    Science.gov (United States)

    Nirogi, Ramakrishna; Kandikere, Vishwottam; Mudigonda, Koteshwara; Ajjala, Devender; Suraneni, Ramakrishna; Thoddi, Parthasarathi

    2011-01-01

    A simple analytical method using liquid chromatography-tandem mass spectrometry (LC-MS/MS) in atmospheric chemical ionization mode (APCI) for the simultaneous estimation of acetylsalicylic acid (ASA, CAS 50-78-2) and its active metabolite salicylic acid (SA, CAS 69-72-7) in human plasma has been developed and validated. ASA and SA were analyzed simultaneously despite differences in plasma concentration ranges of ASA and SA after oral administration of ASA. In spite of having different chemical, ionization and chromatographic properties, ASA and SA were extracted simultaneously from the plasma sample using acetonitrile protein precipitation followed by liquid-liquid extraction. The analytes were separated on a reversed phase column with rapid gradient program using mobile phase consisting of ammonium acetate buffer and methanol. The structural analogue diclofenac was used as an internal standard. The multiple reaction monitoring (MRM) transitions m/z 179 --> 137 for ASA, m/z 137 --> 65 for SA and m/z 294 --> 250 for IS were used. The assay exhibited a linear dynamic range of 0.02-10 microg/mL for ASA and 0.1-50 microg/mL for SA. The between-batch precision (%CV) ranged from 2.1 to 7.9% for ASA and from 0.2 to 5.2% for SA. The between-batch accuracy ranged from 95.4 to 96.7% for ASA and from 94.6 to 111.3% for SA. The validated method was successfully applied for the evaluation of pharmacokinetics of ASA after single oral administration of 650 mg test formulation versus two 325 mg reference formulations of ASA in human subjects.

  14. Acetylsalicylic acid and ascorbic acid combination improves cognition; via antioxidant effect or increased expression of NMDARs and nAChRs?

    Science.gov (United States)

    Kara, Yusuf; Doguc, Duygu Kumbul; Kulac, Esin; Gultekin, Fatih

    2014-05-01

    Chronic inflammation occurs systematically in the central nervous system during ageing, it has been shown that neuroinflammation plays an important role in the pathogenesis of many neurodegenerative disorders. Aspirin, a nonselective COX inhibitor, as well as ascorbic acid, has been purported to protect cerebral tissue. We investigated the effects of subchronic aspirin and ascorbic acid usage on spatial learning, oxidative stress and expressions of NR2A, NR2B, nAChRα7, α4 and β2. Forty male rats (16-18 months) were divided into 4 groups, namely, control, aspirin-treated, ascorbic acid-treated, aspirin+ascorbic acid-treated groups. Following 10-weeks administration period, rats were trained and tested in the Morris water maze. 8-Hydroxy-2-deoxyguanosine and malondialdehyde were evaluated by ELISA and HPLC, respectively. Receptor expressions were assessed by western blotting of hippocampi. Spatial learning performance improved partially in the aspirin group, but significant improvement was seen in the aspirin+ascorbic acid group (p acid group as compared to the control group (p acid in aged rats was shown to enhance cognitive performance and increase the expressions of several receptors related to learning and memory process.

  15. 强酸性阳离子交换树脂催化合成乙酰水杨酸的研究%Synthesis of acetylsalicylic acid using strong-acidic cation-exchange resin as catalyst

    Institute of Scientific and Technical Information of China (English)

    赵志刚; 谢志融; 陈靠山

    2012-01-01

    目的:探讨001×7强酸性阳离子交换树脂催化合成乙酰水杨酸的方法和最佳工艺.方法:通过正交试验探讨了乙酸酐与水杨酸的摩尔比、反应时间、催化剂用量和反应温度对乙酰水杨酸产率的影响,并探讨催化剂的催化能力与使用次数的关系.结果:乙酸酐与水杨酸的摩尔比为3:1、催化剂用量为水杨酸质量的14.50%、反应时间120 min、反应温度60 ℃时,乙酰水杨酸产率最高,为77.93%.结论:001×7强酸性苯乙烯系阳离子交换树脂对酯化反应催化效果好,副反应少,对环境污染小,能重复使用,值得大力推广.%Objective:To optimize the technology of synthesizing acetylsalicylic acid using 001 × 7 strong-acidic cation-exchange resin as catalyst . Methods : Orthogonal experiment was performed to examine the effect of molar ratio of reactants,reaction time, dosage of catalyst, and reaction temperature on the yield of product as well as the efficiency and frequencies of the resin recycled and shifted on the synthesis. Results :The optimal reaction conditions were 3:1 (the ratio of acetic anhydride to salicylic acid,n:n),in a dosage of the resin 14. 50% of salicylic acid,for the reaction time of 120 min at temperature of 60 ℃ , which led to a yield of 77.93 % . Conclusion: 001 × 7 strong-acidic cat ion-exchange resin works well on esterification reaction as a environmentally friendly catalyst and is worthy of wider use, for it has efficient activity, less adverse reaction and recyclable advantages.

  16. Clinical observation on treating cerebral infarction with arasaponin plus acetylsalicylic acid%三七皂甙联合阿司匹林治疗脑梗塞的临床观察

    Institute of Scientific and Technical Information of China (English)

    阎小燕; 崔德芝

    2015-01-01

    目的:探讨三七皂甙联合阿司匹林治疗脑梗塞的临床疗效及安全性。方法:将84例临床诊断为脑梗塞的中老年患者随机分为3组,其中阿司匹林组29例,口服拜阿司匹灵;三七皂甙组27例,口服三七通舒胶囊;三七皂甙联合阿司匹林组28例,联合服用拜阿司匹灵和三七通舒胶囊。比较三组患者的临床疗效,并分析药物安全性。结果:三组患者治疗后神经功能缺损积分与治疗前相比,均显著降低(P<0.01)。III组与I组和II组相比,积分降低显著(P<0.05)。与I组相比,II组、III组PT明显延长,且较I组效果显著(P<0.01)。在PT-INR比较中,三组患者PT-INR均呈现升高的趋势(P<0.01),其中以III组效果最佳,与I组和II组相比有显著性差异(P<0.01)。三组治疗后 D-D、PAgT 水平均明显下降(P<0.01)。I 组患者 PAgT 水平优于 II 组(P<0.05),III组患者PAgT明显低于I组和II组患者(P<0.01)。结论:三七皂甙联合阿司匹林对于抗血小板聚集、颈动脉内膜中层厚度的影响明显优于单用阿司匹林或三七皂甙,且不提高不良反应的发生率,具有良好的疗效性及安全性,为临床抗血栓治疗选择提供依据。%Objective: To discuss the clinical efficacy and safety of the arasaponin plus acetylsalicylic acid on cerebral infarction. Methods: 84 gerontal patients in cerebral infarction were randomly divided into three groups; 29 cases in the acetylsalicylic acid group were given the aspirin treatment; 27 cases in the arasaponin group were given the smooth fluent comfortable panax notoginseng capsule treatment; 28 cases in the arasaponin plus acetylsalicylic acid group were given the aspirin plus the smooth fluent comfortable panax notoginseng capsule treatment. The clinical efficacies in three groups were compared, and analyzed safety of medicine. Results: After treatment, the neurologic deficit score in three

  17. Efeitos da injeção de solução bicarbonatada de ácido acetilsalicílico em mucosa colorretal de coelhos, com vistas a aplicação no preparo pré-operatório do cólon Local effects of rectal washout with acetylsalicylic acid solution on the colonic mucosa of rabbits

    Directory of Open Access Journals (Sweden)

    Enrico Salomão Ioriatti

    2007-12-01

    Full Text Available INTRODUÇÃO: A recidiva local no câncer colorretal tem como principal causa o implante de células tumorais nas anastomoses. 11-15 Dessa maneira, lavagem química do lúmen intestinal é preconizada para evitar tanto o implante quanto à recidiva local. 11-28 Em estudos prévios constatamos que a solução bicarbonatada de ácido acetilsalicílico tem efeitos citolíticos e anti-tumorais in-vitro.31 OBJETIVOS: Avaliar a toxicidade da solução de aspirina na mucosa colônica de coelhos com o objetivo de usá-la no preparo intestinal de portadores de câncer colorretal. MATERIAIS E MÉTODOS: Foram utilizados 20 coelhos. Um clampe vascular foi colocado acima do cólon sigmóide. Os animais foram submetidos a um enema com 50 ml da solução de aspirina ou soro fisiológico de acordo com o grupo. Os animais foram sacrificados ao término do procedimento ou tardiamente de acordo com o grupo. RESULTADOS: A solução de aspirina não altera a mucosa colônica de coelhos. CONCLUSÃO: O uso da solução bicarbonatada de ácido acetilsalicílico no preparo intestinal de portadores de câncer colorretal é clinicamente possível.BACKGROUND: The implantation of viable exfoliated intraluminal tumour cells is the major cause of local recurrence in colorectal cancer. 11-28 Therefore, the bowel lumen wash with a tumoricidal agent has been recommended. 11-28 In previous study we observe that acetylsalicylic acid solution cause neoplastic cell death in vitro.31 PURPOSE: Assess the local effect of acetylsalicylic acid solution on the colonic mucosa of rabbits, in order to use this agent in the bowel lumen wash. METHODS: 20 rabbits were used. A vascular clamp was placed on the distal colon, followed by the instillation per rectum of 50 ml of acetylsalicylic acid solution or saline solution, according to the group. The euthanasia was performed immediately or later according to the group. RESULTS: The acetylsalicylic acid solution doesn't cause any injury on the

  18. Protective effects of levamisole, acetylsalicylic acid, and α-tocopherol against dioxin toxicity measured as the expression of AhR and COX-2 in a chicken embryo model.

    Science.gov (United States)

    Gostomska-Pampuch, Kinga; Ostrowska, Alicja; Kuropka, Piotr; Dobrzyński, Maciej; Ziółkowski, Piotr; Kowalczyk, Artur; Łukaszewicz, Ewa; Gamian, Andrzej; Całkosiński, Ireneusz

    2017-04-01

    Polychlorinated dibenzo-p-dioxins and dibenzofurans (dioxins) are classed as persistent organic pollutants and have adverse effects on multiple functions within the body. Dioxins are known carcinogens, immunotoxins, and teratogens. Dioxins are transformed in vivo, and interactions between the products and the aryl hydrocarbon receptor (AhR) lead to the formation of proinflammatory and toxic metabolites. The aim of this study was to determine whether α-tocopherol (vitamin E), acetylsalicylic acid (ASA), and levamisole can decrease the amount of damage caused by dioxins. Fertile Hubbard Flex commercial line chicken eggs were injected with solutions containing 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) or containing TCDD and the test compounds. The chicken embryos and organs were analyzed after 7 and 13 days. The levels at which AhR and cyclooxygenase-2 (COX-2) proteins (which are induced during inflammation) were expressed were evaluated by performing immunohistochemical analyses on embryos treated with TCDD alone or with TCDD and the test compounds. TCDD caused developmental disorders and increased AhR and COX-2 expression in the chicken embryo tissues. Vitamin E, levamisole, ASA, and ASA plus vitamin E inhibited AhR and COX-2 expression in embryos after 7 days and decreased AhR and COX-2 expression in embryos after 13 days. ASA, levamisole, and ASA plus vitamin E weakened the immune response and prevented multiple organ changes. Vitamin E was not fully protective against developmental changes in the embryos.

  19. 阿司匹林对卵巢癌SKOV3细胞株的增殖和凋亡研究%The Inhibitory Effect of Acetylsalicylic Acid on Ovarian Cancer

    Institute of Scientific and Technical Information of China (English)

    陈颖; 罗剑儒; 魏璐; 唐良萏

    2006-01-01

    目的 观察阿司匹林(acetylsalicylic acid,ASA)对卵巢癌细胞SKOV3增殖和凋亡的影响.方法 采用免疫组化法观察ASA对人卵巢癌细胞系SKOV3中COX-2基因蛋白和癌基因C-erbB-2的表达,流式细胞仪检测ASA对SKOV3细胞周期的影响,透射电镜观察ASA作用SKOV3细胞中凋亡情况.结果 ASA可以明显降低癌基因C-erbB-2在SKOV3细胞中的表达,流式细胞仪结果显示:ASA对SKOV3细胞周期改变有影响,透射电镜发现在ASA作用下的SKOV3细胞有凋亡小体和坏死细胞形成.结论 ASA对卵巢癌SKOV3细胞株具有抑制作用,能够对卵巢癌的防治发挥作用.

  20. Synthesis of Acetylsalicylic Acid by Microwave Irradiation and Analysis of Reaction Kinetics%微波合成乙酰水杨酸及其反应动力学分析

    Institute of Scientific and Technical Information of China (English)

    安从俊; 徐帅; 刘东

    2014-01-01

    采用微波辐射法合成了乙酰水杨酸,考察了反应时间、辐射功率、pH 值、反应底物比(水杨酸与乙酸类衍生物的物质的量比)等因素对反应的影响,并研究了反应动力学。确定最佳反应条件为:反应时间70 s、辐射功率450 W、pH 值5.4、反应底物比1∶2,推算了宏观动力学方程并计算得到表观反应活化能为75.60 kJ·mol-1。%Acetylsalicylic acid was synthesized by microwave irradiation.The effect of several factors,such as reaction time,irradiation power,pH value and reactant ratio(molar ratio of salicylic acid to acetic acid deriva-tive)on reaction were investigated,and reaction kinetics was studied.The optimal conditions were obtained as follows:reaction time of 70 s,irradiation power of 450 W,pH value of 5.4,reactant ratio of 1∶2.The kinetics e-quation was obtained and Arrhenius activation energy was 75.60 kJ·mol-1 .

  1. Content Determination of Acetylsalicylic Acid Essel Cold Tablets by Dual Wavelength Spectrophotometry%双波长分光光度法测定爱索尔感冒片中乙酰水杨酸的含量

    Institute of Scientific and Technical Information of China (English)

    吴雪冬

    2014-01-01

    目的:建立双波长分光光度法测定爱索尔感冒片中乙酰水杨酸的含量的测定方法。方法样品操作及测定方法同重复性试验,平行操作5批样品,另按照中和滴定法测定,比较两种测定方法测定所得样品的百分标示量。结果双波长法:99.2%,97.9%,98.5%,96.5%,98.2%;中和法:100.8%,98.7%,99.8%,97.1%,99.4%。乙酰水杨酸在255nm的波长处有最大吸收,盐酸吗啉胍在250nm的波长附近为225nm波长的等吸收波长,经过精选,选择250.1nm波长为参比波长,225nm波长为测定波长。乙酰水杨酸乙醇溶液放置3h基本稳定,其他成分的乙醇溶液均稳定。结论采用双波长分光光度法测定爱索尔感冒片中乙酰水杨酸的含量,操作简单,所用试剂方便易得,通过两种试验方法的比较,效果较满意。%Objective To establish a method for determination of dual wavelength determination of acetylsalicylic acid essel cold tablets by spectrophotometry. Methods the sample operation and determination method with repeated experiments, paral el operation of 5 batches of samples, determination of the other in accordance with the neutralization titration method, comparison of two determination methods of the sample percent mark. Results The dual wavelength method: 99.2%, 97.9%, 98.5%, 96.5%, 98.2%; neutralization method: 100.8%, 98.7%, 99.8%, 97.1%, 99.4%. Acetyl salicylic acid has a maximum absorption at 255nm wavelength, Moroxydine Hydrochloride absorption wavelength, 225nm wavelength around 250nm wavelength selected, select the 250.1nm wavelength as the reference wavelength, the wavelength of 225nm as the detection wavelength. Acetyl salicylic acid ethanol solution for 3 hours basical y stable, other components are stable in ethanol solution. Conclusion The operation content, determined by double wavelength acetylsalicylic acid essel cold tablets by spectrophotometry is simple, the reagent is convenient and easy, by comparing the two kinds of test

  2. 乙酰水杨酸增强多胺衍生物ANISpm抗肝癌作用及其机制研究%Acetylsalicylic acid strengthens the effects of ANISpm against hepatocellular carcinoma and its molecular mechanism

    Institute of Scientific and Technical Information of China (English)

    谢松强; 张蕾蕾; 杨涛; 马莹; 张亚宏; 李骞; 王建红; 赵瑾; 王超杰

    2011-01-01

    探讨乙酰水杨酸增强多胺衍生物ANISpm抗肝癌作用及其作用机制.采用MTT法检测细胞毒性;应用高内涵活细胞成像系统检测细胞内ANISpm含量的变化及对细胞凋亡和线粒体膜电位的影响;采用Western blotting方法检测细胞色素c,精脒/精胺乙酰转移酶,Caspase-3、-8、-9等蛋白表达的变化;应用高效液相色谱法检测细胞内多胺含量的变化.应用H22肿瘤移植模型评价对实体瘤生长的影响.实验结果显示,乙酰水杨酸体内外均具有增强ANISpm抗肝癌的作用,其机制为乙酰水杨酸通过上调肝癌细胞内精脒/精胺乙酰转移酶的活性,降低细胞内多胺含量从而增加了ANISpm的摄取,并通过ANISpm诱导肝癌细胞凋亡.该凋亡作用与ANISpm诱导细胞线粒体膜电位降低,促进细胞色素c释放以及活化Caspase-3、-8、-9等有关.%The objective of this study is to examine the effects of ANISptn, a novel polyamine naphthalimide conjugate, with acetylsalicylic acid against hepatocellular carcinoma in vivo and in vitro and elucidate its potential molecular mechanism. The proliferation inhibition was detected by MTT assay. Cell apoptosis, intracellular fluorescence intensity and mitochondrial membrane potential (MMP) were detected by high content screening (HCS) analysis. Polyamines content was analyzed by reverse-phase high performance liquid chromatography. Protein expression levels were quantified by Western blotting assay. The combination treatment strongly inhibited cell proliferation, induced cell apoptosis in HepG2 cells and H22 hepatoma cells, which was mediated by enhanced ANISpm uptake via up-regulation of spermidine/spermine N1-acetyltransferase (SSAT) and depression of intracellular polyamine. Furthermore, this synergistic apoptosis was involved in mitochondria and death-receptor signal pathway. All these findings demonstrated that the combination treatment with acetylsalicylic acid and ANISpm resulted in synergistic

  3. Desensitization to acetyl-salicylic acid as a treatment for non-steroid anti-inflammatory drugs (NSAIDs-exacerbated respiratory disease = Desensibilización al ácido acetil-salicílico como tratamiento para la enfermedad respiratoria exacerbada por antiinflamatorios no esteroides

    Directory of Open Access Journals (Sweden)

    Cardona Villa, Ricardo

    2014-07-01

    Full Text Available Desensitization to acetyl-salicylic acid as a treatment for non-steroid anti-inflammatory drugs (NSAIDs-exacerbated respiratory disease The coexistence of hypersensitivity to acetylsalicylic acid (ASA and other NSAIDs with disease of the upper or the lower airways (rhinosinusitis/sinonasal polyposis, or asthma is defined as NSAIDs-exacerbated respiratory disease. Treatment options include the avoidance of all analgesics that inhibit COX-1 or ASA desensitization, continuing its daily consumption. The latter treatment has shown to improve quality of life, reduce the formation of sinonasal polyps, the episodes of sinus infection, the frequency of hospitalizations and surgeries for resection of polyps and the need for systemic steroid treatment. Multiple desensitization schedules have been used, trying to reduce the risk associated with the procedure and the adverse effects of chronic use of ASA. In this paper we present a review of the different methods of desensitization and two illustrative clinical cases to help understand the factors that influence the choice of treatment for these patients.

  4. 乙酰水杨酸分子印记聚合物的合成条件研究∗%Study on Polymerization Conditions for Molecularly Imprinted Polymers Using Acetylsalicylic Acid as Template

    Institute of Scientific and Technical Information of China (English)

    赵丹丹; 陈盛余; 李丽; 史兵方; 彭龙基

    2016-01-01

    采用分子印迹技术,以乙酰水杨酸为模板分子,丙烯酰胺为功能单体,乙二醇二甲基丙烯酸酯为交联剂,偶氮二异丁腈为引发剂合成乙酰水杨酸分子印迹聚合物。考察了单体与交联剂比例、引发剂用量、溶剂用量、反应时间和反应温度对特异性吸附量的影响,结果表明:在乙酰水杨酸为0.181 g,丙烯酰胺为0.285 g,交联剂为6.94 g,引发剂为100 mg,溶剂用量为20 mL,反应温度为65℃,反应时间为18 h的条件下,聚合物有较好吸附效果。制备的印迹聚合物对乙酰水杨酸的特异性吸附量为17.7 mg/g。%The molecular imprinted polymer ( MIP ) was synthesized by precipitation polymerization with acetylsalicylic acid ( Asp ) as template, acrylamide ( AM ) as functional monomer, ethylene glycol dimethacrylate ( EGDMA) as crosslinker and Azo-iso-butyronitrile ( AIBN) as initiator. The factors of influence such as the ratio of monomer to crosslinker, the amount of initiator, the amount of solvent, the reaction time and the reaction temperature were investigated. The results showed that the optimum reaction conditions were obtained as follows: the amount of crosslinker was 6. 94 g, the amount of initiator was 100 mg, the amount of solvent was 20 mL, the reaction time was 65℃and the reaction time was 18 h when the amount of Asp was 0. 181 g and acrylamide was 0. 285 g. The adsorbing capacity of MIP which had specific molecule recognition ability to Asp was 17. 7 mg/g.

  5. 磷钨钼杂多阴离子柱撑水滑石的制备及催化合成乙酰水杨酸%Tungstomolybdophosphate heteropolyanions pillared layered double hydroxides (LDHs) :preparation and catalytic systhesis of acetylsalicylic acid

    Institute of Scientific and Technical Information of China (English)

    林文权; 王力耕; 袁庭; 施炜; 倪哲明

    2011-01-01

    Three kinds of tungstomolybdophosphate heteropolyanions [PWχMo12-χO40]3- (χ=l, 3,6) pillared layered double hydroxides (LDHs) were prepared by ion exchange using NO3 - LDHs as a precursor. The materials prepared were characterized by XRD and FT-IR . The catalytic activity were further investigated in the synthesis of acetylsalicylic acid with salicylic acid and acetic anhydride as materials. The results showed that [PWχMo12-χO40]3- (χ = 1,3,6) could totally replace the original interlayer nitrate anions of the NO3-LDHs, producing PWχMo12-χ- LDHs (χ=l,3,6) with good crystallinity. And the PWMo11-LDHs catalyst has high catalytic activity. The optimum reaction conditions for the catalytic synthesis of acetylsalicylic acid on the PWMo11-LDHs catalyst were obtained as follows: the reaction time was 10 min, the reaction temperature was 75℃, the molar ratio of salicylic acid to acetic anhydride was 1:2, the amount of catalyst was equal to 10% salicylic acid. Under these conditions, the yield of acetylsalicylic acid reached 82.02%.%以NO3-LDHs水滑石为前躯体,用离子交换法将三种磷钨钼杂多阴离子[PWxMo12-xO40]3-(x=1,3,6)柱撑到水滑石层间,用XRD和FT-IR方法对样品进行了表征.并以水杨酸和乙酸酐为原料,考察了催化剂合成乙酰水杨酸的催化活性.结果表明:[PWxMo12-xO40]3- (x=1,3,6)已完全取代了前体水滑石中NO3-进入水滑石层间,得到晶相良好的PWxMo12-x-LDHs(x=1,3,6).其中PWMo11-LDHs催化剂具有催化活性高,其最佳催化合成条件:反应时间10 min,反应温度75℃,水杨酸与乙酸酐摩尔比为1:2,催化剂用量为水杨酸质量的10%,乙酰水杨酸收率达82.02%.

  6. Effect of ultrasonic irradiation on the number of acetylsalicylic acid crystals produced under the supersaturated condition and the ability of controlling the final crystal size via primary nucleation

    Science.gov (United States)

    Miyasaka, Etsuko; Kato, Yumi; Hagisawa, Minoru; Hirasawa, Izumi

    2006-03-01

    The purposes of this study were to investigate the effects of ultrasound irradiation on the number of crystals formed in an acetylsalicyclic acid crystallization process and to assess the controllability of the final product size via the number of primary nuclei. The number of crystals present after primary nucleation was counted and the relationship between the final product size and the number of crystals was examined. Additionally, the growing ASA crystals were observed, since ultrasound energy not only may control primary nucleation but may also the perfection of the crystal shape. At a high level of ultrasonic energy, ultrasound irradiation increased the average number of crystals, an effect that has been reported often; however, at a low level of ultrasonic energy it decreased the average number of crystals, and moreover, these opposing ultrasonic effects on the number of crystals interchanged at a specific energy threshold. These results reveal two novel phenomena—that there is an energy region where ultrasonic irradiation inhibits primary nucleation, and that a specific amount of ultrasonic energy is needed to activate primary nucleation. On the other hand, the final product size almost depended upon the number of primary nuclei, indicating that the final product size could be controlled via the number of crystals influenced by ultrasound irradiation. According to the photographs of crystals, they were not destroyed by the process. Therefore, it was proposed that ultrasound energy does not destroy the perfection of the crystal shape but only controls primary nucleation under the condition: both short irradiation time and low supersaturated condition.

  7. Preparation and characterization of H6P2W18O62/Kaolin and its activity on the catalytic synthesis of acetylsalicylic acid%H6P2W18O62/高岭土的制备、表征及催化合成乙酰水杨酸

    Institute of Scientific and Technical Information of China (English)

    曹小华; 王原平; 徐常龙; 雷艳虹; 占昌朝

    2014-01-01

    H6P2W18O62/kaolin was fabricated by dipping Kaolin in the mixing solution of phosphotungstic acid with Dawson structure,and characterized by FT-IR,XRD,SEM and EDS. The catalytic synthesis of acetylsalicylic was carried out as a probe reaction to study the acid catalytic performance of the catalyst,under the optimal condition,i.e. the supported quantity of 40%,w (catalyst)=7.2%(relative to the dosage of salicylic acid),reaction temperature of 90℃,and reaction time of 40min. The average yield of acetylsalicylic acid reaches 90.2%. The catalyst shows good reusability. After its five time usage,the yield of acetylsalicylic acid was still above 85.1%. The catalyst is attractive for esterification by its low cost,high activity,simple post-treatment,no corrosion to the equipment and no pollution.%以高岭土为载体,Dawson结构磷钨酸(H6P2W18O62·13H2O)为活性组分制备了负载型催化剂H6P2W18O62/高岭土,并通过FT-IR、XRD、SEM和EDS对催化剂进行表征。以催化合成乙酰水杨酸为探针反应,考察了催化剂的酸催化性能。结果表明,在优化反应条件为H6P2W18O62负载量为40%,w(H6P2W18O62/高岭土)=7.2%(基于水杨酸的质量),反应温度为90℃,反应时间为40min时,乙酰水杨酸收率达90.2%,催化剂重复使用5次,乙酰水杨酸收率仍可达到85.1%。该催化剂具有价廉易得、催化活性高、后处理工艺简单、不腐蚀设备、无环境污染、可重复使用等优点。

  8. Effects of acetylsalicylic acid and acetic acid solutions in VX2 carcinoma cells: In vitro analysis Efeito da solução de ácido acetilsalicílico e de ácido acético sobre o carcinoma vx-2: Análise in vitro

    Directory of Open Access Journals (Sweden)

    Rogério Saad-Hossne

    2006-06-01

    Full Text Available PURPOSE: To analyze, in vitro, the effects of acetylsalicylic acid (aspirin and acetic acid solutions on VX2 carcinoma cells in suspension and to examine the correlation between these effects and neoplastic cell death. METHODS: The VX2 tumor cells (10(7 cells/ml were incubated in solutions containing differing concentrations (2.5% and 5% of either acetylsalicylic acid or acetic acid, or in saline solution (controls. Every five minutes, cell viability was tested (using the trypan blue test and analyzed under light microscopy. RESULTS: Tumor cell viability (in % decreased progressively and, by 30 minutes, neoplastic cell death had occurred in all solutions. CONCLUSION: Based on this experimental model and the methodology employed, we conclude that these solutions cause neoplastic cell death in vitro.OBJETIVO: Analisar os efeitos das soluções de ácido acetil salicílico (aspirina e de ácido acético, in vitro, sobre células em suspensão do carcinoma VX-2, verificando-se as mesmas causam a morte das células neoplásicas. MÉTODOS: Procedeu-se a incubação das células tumorais VX-2 (10(7 células/ml com diferentes concentrações do ácido acetil salicílico (2,5% e 5% e de ácido acético (2,5% e 5%, sendo estudada a viabilidade celular pelo teste do azul tripian a cada 5 minutos; procedeu-se à análise à microscopia ótica. RESULTADOS: Observou-se que o percentual de viabilidade das células tumorais foi progressivamente diminuindo, sendo que ao final de 30 minutos todas as células neoplásicas estavam inviáveis em todas as soluções e concentrações utilizadas. CONCLUSÃO: Com base neste modelo experimental e com a metodologia empregada, concluiu-se que in vitro, estas soluções causam a morte (inviabilidade das células neoplásicas.

  9. [Therapeutic use of acetylsalicylic acid in diabetics].

    Science.gov (United States)

    Zácková, V

    2003-12-01

    Aterosclerosis is a leading cause of morbidity and mortality in diabetics. Macrovascular diseases--myocardial infarction, cerebral vascular accident, ischemic lower extremities--start in persons with diabetes earlier and in a bigger scope then in non-diabetics. Development of these changes is determined by diabetic vasculopathy which is connected with endothelial dysfunction, hypercoagulation state, and platelet abnormalities. Treatment of a patient with diabetes is based on compensation of diabetes and management of hypertension and dyslipidaemia. Drugs that inhibit platelets constitute an important part of prevention of cardiovascular disabilities in diabetics.

  10. [Clopidogrel plus acetylsalicylic acid: a deadly combination

    NARCIS (Netherlands)

    Rongen, G.A.P.J.M.

    2013-01-01

    In the recently published SPS3 trial, clopidogrel plus aspirin increased mortality compared with aspirin alone in patients with lacunar cerebral infarcts. A detailed review of currently available trial data on this dual-antiplatelet strategy, having taken the between-trial variation in mortality in

  11. [Interaction between NSAIDs and acetylsalicylic acid disregarded

    NARCIS (Netherlands)

    Vollaard, E.J.; Kramers, C.; Brouwers, J.R.B.J.

    2014-01-01

    In 2013 the European Medicines Agency declared that diclofenac is contraindicated in patients with arterial thrombotic complications, based on a meta-analysis of randomised controlled trials on the adverse reactions of NSAIDs. The same decision was taken for coxibs some years earlier. The Dutch auth

  12. 糊精对乙酰水杨酸肠溶片含量测定的影响%Effect of Dextrin on Determination for Acetylsalicylic Acid Enteric-coated Tablets

    Institute of Scientific and Technical Information of China (English)

    翁水旺; 周继斌

    2001-01-01

    The method for content determination of acetylsalicylic acidenteric-coated tablet was studied. The influence of auxiliary materials may be eliminated when main ingredients are determined after tablets dissolved in alcohol and filtered. The average recovery was 100.2%, and RSD was 0.17%. The method is simple and accruate.%探讨小剂量乙酰水杨酸肠溶片的含量测定方法。将原方法改为全用乙醇溶解、定容并滤过后进行测定,可排除辅料糊精对主药测定的干扰。方法平均回收率为100.2%,RSD为0.17%。修改后的方法简便、准确。

  13. Effects of acetylsalicylic acid and acetic acid solutions on VX2 liver carcinoma in rabbits: in vivo analysis Efeitos das soluções de aspirina e de ácido acético em fígado de coelhos portadores de tumor hepático VX2: análise in vivo

    Directory of Open Access Journals (Sweden)

    Rogério Saad-Hossne

    2007-08-01

    Full Text Available PURPOSE: To analyze, in vitro, the effects of acetylsalicylic acid (aspirin and acetic acid solutions on VX2 carcinoma cells in the liver of rabbits with VX2 hepatic tumors; to determine the histolytic and anatomopathological characteristics of the solutions; and to evaluate the eventual biochemical and hepatic changes. METHODS: A total of 48 rabbits were evaluated. The animals were randomized into two groups, protocol 3 (study group and protocol 4 (controls, and each group was then subdivided into 3 subgroups. Four days after implantation of the tumor in the liver, median laparotomy was performed with a 0.4-ml injection of a solution of either aspirin (5.0%, acetic acid (5.0% or saline. The animals were sacrificed after 24 hours (protocol 3 or after 11 days (protocol 4. Body weight, clinical evolution and biochemical levels, as well as the abdominal and thoracic cavities, were evaluated, and liver microscopy was performed. RESULTS: No changes in clinical evolution, body weight or biochemical levels were reported. However, an increase in alkaline phosphatase was observed in protocol 4 (controls. The tumor was eliminated in both protocols. CONCLUSION: Acetylsalicylic acid and acetic acid solutions cause the destruction of experimental hepatic tumors.OBJETIVO: Analisar os efeitos das soluções de aspirina e de ácido acético, in vivo, em fígado de coelhos portadores de tumor hepático VX2, verificando o efeito histolítico e anatomo-patológico das soluções e eventuais alterações bioquímicas hepáticas. MÉTODOS: Utilizou-se 48 coelhos, divididos em 2 protocolos experimentais(3 e 4, subdivididos em 3 grupos cada. Após 4 dias da implantação do tumor no fígado, procedeu-se a laparotomia mediana, com injeção de 0,4 ml da solução de aspirina (5,0%, de ácido acético (5,0% e solução salina; o sacrifício ocorreu apos 24 horas (protocolo 3 e 11 dias (protocolo 4; avaliou-se o peso, evolução clinica, dosagens bioquímicas, cavidade

  14. Estudo comparativo entre agregação plaquetária por turbidimetria e impedância elétrica em pacientes sob terapia antiplaquetária à base de ácido acetilsalicílico Comparative study of platelet aggregation by turbidimetric and impedance methods in patients under acetylsalicylic acid antiplatelet therapy

    Directory of Open Access Journals (Sweden)

    Leonardo Lorenzo da Silva

    2010-01-01

    Full Text Available INTRODUÇÃO: A hiperagregação (agregação excessiva das plaquetas pode causar a formação de um trombo e a posterior oclusão dos vasos sanguíneos levando à isquemia. Esse fenômeno é responsável por doenças isquêmicas cardiovasculares, como angina pectoris e aterosclerose, bem como outras formas de isquemia, como o acidente vascular cerebral. Visando diminuir a função das plaquetas para reduzir a formação de trombos, o ácido acetilsalicílico vem sendo utilizado para tratamento antitrombótico, com diversos estudos mostrando sua eficácia. Dessa forma faz-se mister o uso de uma ferramenta laboratorial para o monitoramento da efetividade do tratamento, o que é feito por meio do teste de agregação plaquetária. O objetivo desse estudo foi comparar duas metodologias para esse exame (impedância elétrica e turbidimetria em relação a trinta pacientes adultos de ambos os sexos em uso do fármaco. CONCLUSÃO: Os resultados mostraram uma boa correlação entre os métodos, possibilitando o uso concomitante de ambas as técnicas em laboratórios clínicos de rotina.INTRODUCTION: Hyperaggregation of platelets can cause the formation of thrombi and subsequent occlusion of blood vessels leading to ischemia. This phenomenon can be responsible for ischemic cardiovascular diseases such as angina pectoris and atherosclerosis as well as other forms of ischemia such as stroke. To decrease platelet function and reduce the formation of thrombi, acetylsalicylic acid has been used for antithrombotic treatment, with several studies showing its effectiveness. Therefore it is necessary to use a laboratory tool to monitor the effectiveness of treatment, which is achieved through laboratory testing of platelet aggregation. The aim of this study was to compare two different methods (impedance and turbidimetry to test platelet aggregation in 30 adult patients of both genders taking acetylsalicylic acid. CONCLUSION: The results show that there is a

  15. Acetylsalicylic Acid (aspirin) in Vitro Inhibition of Influenza Virus H1N1%乙酰水杨酸(阿司匹林)体外对流感病毒H1N1的抑制作用

    Institute of Scientific and Technical Information of China (English)

    丁宁; 卢芯; 郑丛龙; 韦淳巍; 许梦亭; 向敏; 林雨馨

    2014-01-01

    探讨乙酰水杨酸(Acetylsalicylic Acid)在体外对流感病毒H1N1的抑制作用。采用血球凝集试验、神经氨酸酶活性抑制试验和鸡胚接种法,观察AS对流感病毒H1N1的抑制作用。血球凝集试验可以看出,AS对流感病毒H1N1包膜表面的血凝素活性有一定的抑制作用,且作用较为显著;鸡胚培养法的结果显示,AS明显抑制了流感病毒H1N1在鸡胚内的增值,实验组血凝效价低于1:2,对照组血凝效价为1:512;神经氨酸酶活性抑制试验的结果显示,AS能够明显抑制流感病毒H1N1的神经氨酸酶活性。结果表明AS在体外对流感病毒H1N1有明显的抑制作用,其抑制机理可能与AS对流感病毒血凝素和神经氨酸酶活性抑制有关。%To study the acetylsalicylic acid (AS) in vitro inhibition of influenza virus H1N1. Using methods of hemagglutination test, neuraminidase enzyme inhibition test and chicken embryo inoculation, the inhibition of influenza virus H1N1 was observed. Hemagglutination test results showed that AS inhibited activity of the H1N1 influenza virus hemagglutinin and the effect is more significant; embryo culture results showed, AS significantly inhibited H1N1 influenza virus in eggs value within the experimental group hemagglutination titer less than 1:2, the control group hemagglutination titer 1:512;neuraminidase enzyme inhibition test results showed, AS can inhibit the influenza virus H1N1 neuraminidase activity. All study showed that H1N1 influenza virus in vitro was significantly inhibited by AS, the mechanism is concern with AS inhibition of influenza virus hemagglutinin and neuraminidase inhibition of enzyme activity.

  16. UPLC - MS/MS法测定比格犬血浆中阿司匹林、水杨酸和单硝酸异山梨酯的浓度%UPLC-MS/MS determination of acetylsalicylic acid, salicylic acid and isosorbide-5-mononitrate in dog plasma

    Institute of Scientific and Technical Information of China (English)

    向志雄; 刘海燕; 孙星; 徐佳珺; 刘文丽

    2012-01-01

    目的:建立灵敏的超高效液相色谱-质谱联用法测定比格犬血浆中的阿司匹林、水杨酸和单硝酸异山梨酯的浓度.方法:选用Waters BEH C18(100 mm ×2.1 mm,1.7 μm)色谱柱,分别以0.5%甲酸/5 mmol· L-1醋酸铵-乙腈和2 mmol·L-1醋酸铵-乙腈为流动相,采用梯度洗脱进行分离,样品采用乙酸乙酯提取后进样,通过电喷雾电离源,以多重反应监测(MRM)方式进行负离子检测,用于定量分析的离子对分别为m/z 178.9→136.9(阿司匹林)、m/z 136.9→64.9(水杨酸)和m/z 293.7→250.0(内标,双氯酚酸钠)测定阿司匹林和水杨酸;m/z 249.6→58.9(单硝酸异山梨酯)和m/z 293.7→250.0(内标,双氯酚酸钠)测定单硝酸异山梨酯.结果:阿司匹林、水杨酸和单硝酸异山梨酯的线性范围分别为2.0 ~ 2000.0,20.0 ~ 16000.0,9.6 ~9557.0 ng·mL-1;定量下限分别可达2.0,20.0,9.6 ng·mL-1;日内、日间精密度(RSD)均小于15%.结论:本方法灵敏度较高,血浆用量少,适用于比格犬血浆样品中阿司匹林、水杨酸和单硝酸异山梨酯的测定和药物动力学研究.%Objective:To develop an UPLC - MS/MS method for determination of acetylsalicylic acid( ASA) and its metabolite(salicylic acid,SA) ,isosorbide -5 - mononitrate(5 -ISMN) in dog plasma. Methods; The dog plasma was extracted by ethyl acetate,and separated on a BEH C18(100 mm × 2. 1 mm,l. 7μm) column by gradient elu-tion using acetonitrile -0. 5% formic acid -5 mmol · L-1 ammonium acetate and acetonitrile -2 mmol · L-1 ammonium acetate as mobile phases respectively. A tandem mass spectrometer equipped with electrospray ionization source was adopted as the detector. Multiple reaction monitoring ( MRM ) transitions of m/z 178. 9→-136. 9, m/z 136. 9→64. 9,m/z 249. 6→58. 9 and m/z 293. 7→250. 0 were measured in negative mode for ASA,SA,5 - ISMN and internal standard,respectively. Results;The linear concentration ranges of the calibration curve for ASA,SA, 5

  17. Synthesis, spectral properties and thermal behaviour of zinc(II) acetylsalicylate

    Energy Technology Data Exchange (ETDEWEB)

    Lambi, John N.; Nsehyuka, Alfred T.; Egbewatt, Nkongho; Cafferata, Lazaro F.R.; Arvia, Alejandro J

    2003-03-05

    The thermal behaviour of zinc(II) acetylsalicylate [Zn(acsa){sub 2}(H{sub 2}O){sub 2}] with respect to phase transitions, pyrolysis both in air and inert (N{sub 2}) atmosphere, and product identification has been investigated. The complex was synthesised by metathesis in hot ethanol solution using aspirin (acetylsalicylic acid) as precursor and characterised via electronic and IR spectral analyses. Optical observations showed that the white salt does not undergo a direct transition from the solid to the liquid phase but rather goes slowly through an intermediate mesophase around 80 deg. C before melting rapidly to the brick-brown isotropic liquid around 134-136 deg. C. No liquid crystalline phases are however formed. This result was complemented by that from thermogravimetric (TG) studies in the ca. 25-600 deg. C range, which showed three main weight-loss phases of 8.0, 50.0 and 14.0% (around 200, 250 and 400 deg. C) corresponding, respectively, to the elimination of CO{sub 2}, xanthone and acetic acid. The pyrolysis products, as identified using a combination of instrumental (GC-MS) and wet chemical techniques are: CO{sub 2}; non-stoichiometric zinc oxide, most likely in the form: Zn{sub 1+x}O (where 0.0000{<=}x{<=}0.0003); and a mixture of organic products resulting from further decomposition, charring and other attendant thermal effects at the relatively high temperatures (ca. 600 deg. C) involved. Six of the principal organic products were identified and included salsalate and benorylate which are pro-drugs of salicylic acid, a well-known pharmaceutical.

  18. 采前乙酰水杨酸与采后1-MCP处理对厚皮甜瓜冷藏品质及抗氧化能力的影响%Effect of Preharvest Acetylsalicylic Acid and Postharvest 1-MCP Treatments on Quality and Antioxidant Ability of Muskmelon Fruit during Cool Storage

    Institute of Scientific and Technical Information of China (English)

    尚琪; 王婷; 李欣; 刘耀娜; 白晓东; 张溪桐; 王毅; 毕阳

    2016-01-01

    以“玛瑙”厚皮甜瓜为试材,通过采前分别在幼果期(花后2周)、膨大期(花后3周)、网纹形成期(花后4周)和采前2 d 4个时期喷洒乙酰水杨酸和采后1-甲基环丙烯(1-methylcyclopropene,1-MCP)熏蒸,研究单独或复合处理对冷藏期间果实品质及抗氧化能力的影响。结果表明,采前乙酰水杨酸处理可有效抑制贮藏期间果实的质量损失率的增加,延缓果皮转黄,维持可溶性固形物和可滴定酸含量,提高总酚和类黄酮含量,提高抗氧化能力。1-MCP熏蒸能减少果实采后质量损失,维持硬度,增加抗坏血酸含量。复合处理在维持果实可溶性固形物和可滴定酸含量、提高总酚和类黄酮的含量方面表现出协同效应。由此表明,乙酰水杨酸和1-MCP处理对维持甜瓜果实采后品质的作用效果与抑制乙烯的产生有关,而果实抗氧化能力的提高则与促进苯丙烷代谢产物及抗坏血酸的积累相关。%This study examined effects of multiple preharvest acetylsalicylic acid (ASA) sprays combined with postharvest 1-methylcyclopropene (1-MCP) fumigation on the quality and antioxidant ability of muskmelon (Cucumis melo cv. Manao) fruit during cool storage. The plants were sprayed with ASA four times, namely at young fruit period (2 weeks after lfowering), fruit enlarging period (3 weeks after lfowering), netting period (4 weeks after lfowering) and 2 days before harvest, respectively. After harvest, the fruits were fumigated with 1-MCP. The results indicated that preharvest ASA treatment inhibited weight loss, retarded peel yellowing, maintained the levels of total soluble solids and titratable acid, increased the contents of total phenolics and lfavonoids, and enhanced the antioxidant ability of fruits. 1-MCP fumigation decreased weight loss, maintained fruit ifrmness and increased the contents of ascorbic acid. Preharvest ASA combined with postharvest 1-MCP

  19. 埃索美拉唑在预防老年人阿司匹林相关性溃疡中的作用%The effect of esomeprazole in prevention of peptic ulcers in old patients treated with low-dose of acetylsalicylic acid

    Institute of Scientific and Technical Information of China (English)

    刘兰; 苟晓; 窦德才; 王倩; 陈俪

    2013-01-01

    Objective To determine whether 40 mg of esomeprazole daily reduces the incidence of peptic ulcers over 12 weeks of treatment in patients taking low-dose acetylsalicylic acid (ASA). Methods From January 2010 to December 2012, 242 cases of Helicobacter pylori-negative patients who took a low dose of ASA everyday were included. These patients were randomly divided into esomeprazole group and control group. Esomeprazole group was treated with 40 mg of esomeprazole once a day for 12 weeks, and the control group with placebo. The patients were confirmed peptic ulcer by endoscopy at the end of the treatment. Results After 12 weeks, we found that esomeprazole group significantly reduced the proportion of patients at the risk of peptic ulcers and csomeprazole was generally well tolerated. Conclusion Acid-suppressive treatment with esomeprazole 40 mg a day reduced the occurrence of peptic ulcers in patients at risk for ulcer development who were taking low-dose ASA.%目的 观察埃索美拉唑在降低低剂量阿司匹林治疗的老年人中相关溃疡发病率的作用.方法 纳入需长期低剂量服用阿司匹林的患者242例,均经快速尿素酶法检测确认无现症幽门螺杆菌感染,符合纳入标准和不具备排除标准的病人,按奇偶数原则和1:1比例随机分配进入埃索美拉唑组和对照观察组.治疗组晨起餐前口服埃索美拉唑胶囊40mg,每天1次;对照组口服硫糖铝混悬液10ml,每天2次.所有病人观察期限为12周,观察终点后所有纳入研究的病人均需复查胃镜.结果 治疗组中无一例出现阿司匹林相关性溃疡及其他上消化道症状,对照组中有11例出现黑便,7例粪便隐血阳性,5例血红蛋白降低(Hb<10g/ml),5例出现消化性溃疡.结论 埃索美拉唑40 mg/d可以有效降低服用低剂量ASA患者发生内镜下可见消化性溃疡的风险,值得在临床推广.

  20. Aspirin (acetylsalicylic acid) effects on behavioral thermoregulation with microwave radiation.

    Science.gov (United States)

    Vitulli, W F; Laconsay, K L; Agnew, A C; Henderson, M E; Quinn, J M; Holland, B E; DePace, A N

    1993-08-01

    Aspirin is a widely used over-the-counter drug in our society which has wide therapeutic value, yet not all of the behavioral side effects have been studied. Different doses of aspirin solutions were administered (ip) prior to fixed-interval 2-min. schedules of microwave reinforcement in rats tested in a cold environment. Four Sprague-Dawley rats were conditioned to regulate their thermal environment with 5-sec. exposures of MW reinforcement. Friedman's nonparametric test showed significant differences among aspirin and saline-control doses. Post hoc sign tests showed that a moderate dose of aspirin increased operant behavior reinforced by MW radiation, yet lower and higher doses decreased and then increased the rate of responding which resulted in an inverted U-shaped trend. Possible multiple effects of aspirin in terms of its thermoregulatory as well as its pain-tolerance properties, and implications for hypothalamic "set point" are discussed.

  1. Acetylsalicylic acid and morphology of red blood cells

    Directory of Open Access Journals (Sweden)

    Jacques Natan Grinapel Frydman

    2010-06-01

    Full Text Available This work evaluated the effect of in vitro and in vivo treatment with ASA on the morphology of the red blood cells. Blood samples or Wistar rats were treated with ASA for one hour. Blood samples or animals treated with saline were used as control group. Blood smears were prepared, fixed, stained and the qualitative and quantitative morphology of red blood cells were evaluated under optical microscopy. Data showed that the in vitro treatment for one hour with ASA at higher dose used significantly (pEste trabalho avaliou o efeito do tratamento in vitro e in vivo com AAS na morfologia dos eritrócitos. Amostras de sangue ou ratos Wistar foram tratadas com AAS por uma hora. Amostras sangüíneas ou animais tratados com salina foram utilizados como grupos controle. Distensões de sangue foram preparadas, fixadas, coradas e a análise morfológica qualitativa e quantitativa dos eritrócitos foi realizada em microscópio óptico. Os dados mostraram que o tratamento in vitro por uma hora com AAS na maior dose utilizada modificou significativamente (p<0.05 a relação perímetro/área dos eritrócitos. Não foram obtidas alterações morfológicas com o tratamento in vivo. O uso do AAS em doses altas poderia interferir na forma dos eritrócitos.

  2. [Correlation between the output and composition of essential oil and the level of salicylic acid in mint plants at different ontogenetic stages].

    Science.gov (United States)

    Shelepova, O V; Kondrat'eva, V V; Voronkova, T V; Olekhnovich, L S

    2013-01-01

    Dynamic changes in the content of acetylsalicylic acid and the output and qualitative composition of essential oil have been studied in mint plants (Mentha spicata L. and cultivar Medichka) during their ontogenesis with allowance for changes in weather conditions. Ontogenetic changes in the level of acetylsalicylic acid in leaf tissues are found to be similar in both cv. Medichka and M. spicata. In the case of cv. Medichka, this change is connected with the dynamics of the production and the qualitative composition of essential oil; in the case of M. spicata, this connection is less expressed. The role of acetylsalicylic acid and essential oil in plant adaptation to the environment is discussed.

  3. Efeito da solução de ácido acetilsalicílico e de ácido acético em fígado de coelhos Effect of acetylsalicylic acid and acetic acid solutions in liver of rabbits

    Directory of Open Access Journals (Sweden)

    Rogério Saad-Hossne

    2004-12-01

    Full Text Available Objetivo: Analisar os efeitos das soluções de aspirina e de ácido acético, in vivo, em fígado de coelhos sadios, verificando o efeito histolítico e o resultado anatomo-patológico das lesões e eventuais alterações bioquímicas hepáticas. Métodos: Utilizou-se 80 coelhos, divididos em 2 protocolos experimentais (1 e 2, subdivididos em 5 grupos cada, sendo os mesmos submetidos a laparotomia mediana, com injeção de 0,4 ml da solução de aspirina (2,5 e 5,0%, de ácido acético (2,5 e 5,0% e solução salina; o sacrifício ocorreu apos 24 horas (protocolo1 e 14 dias (protocolo 2; avaliou-se o peso, evolução clinica, dosagens bioquímicas, cavidade abdominal e torácica e microscopia do fígado. Resultados: Não foram observadas alterações na evolução clinica, peso e nas dosagens bioquímicas, apenas elevação da AST e ALT no grupo 24 horas(Protocolo 1. À macroscópica mostrou que nos animais tratados, em ambos os grupos, a presença de lesão hepática localizada na área infiltrada, correspondente a necrose (24 horas e fibrose (14 dias. Conclusão: Ambas as soluções (aspirina e ácido acético acarretaram destruição localizada do órgão substituída por fibrose apos 14 dias.Purpose: In the present work, 2.5% and 5% acetyl salicylic acid solution and acetic acid solutions were tested in vivo. Methods: In all tests control animals were used and given salt solution. 80 male rabbits were employed and randomly distributed among the different experimental groups. Results: When injected in the liver of healthy rabbits (in vivo, both solutions produced localized destruction (coagulative necrosis of the hepatic parenchyma in 24 hours. After 14 days, these lesions either disappeared or were replaced by mild scars (fibrosis. The lesions were not followed by clinical alterations and the only observed biochemical alteration was an increase in the amount of alanine amino transferase after 24 hours. Conclusion: In vivo, the effects of

  4. Surfactant and Gelation Properties of Acetylsalicylate Based Room Temperature Ionic Liquid in Aqueous Media.

    Science.gov (United States)

    Sastry, Nandhibatla V; Singh, Dipak K

    2016-10-04

    An amphiphilic room temperature ionic liquid (RTIL) containing acetylsalicylate anion of type 1-dodecyl-1-methylpiperidinium acetylsalicylate, [C12mpip][AcSa], is synthesized from the precursor [C12mpip][Cl] by an ion exchange process. The sample is characterized, and its surface active and aggregation behavior in water has been studied and explained. The critical aggregation concentrations (CACs) are determined by a variety of methods, namely, electrical conductivity, surface tension, steady state florescence, and isothermal titration calorimetry (ITC) at different temperatures. As compared to its precursor, [C12mpip][AcSa] has low CAC values, indicating enhanced favorable interactions between the [alkylmpip](+) cation···bulky [AcSa](-) anion and also hydrogen bonding of both of the ions with water. The free energy of aggregation ΔG(0)a is always negative, and both enthalpy and entropy of aggregation drive the aggregation process. The micelle-like aggregates are ellipsoidal in shape. The aggregation numbers are determined from translational diffusion coefficients and florescence quenching measurements. Aggregates of [C12mpip][AcSa] are larger than those of its precursor IL with chloride anion. Therefore, it is evident that the close interactions between the ion pairs of [C12mpip](+)···[AcSa](-) facilitate packing of more molecules in an aggregate. The steady state and oscillatory rheology measurements in aqueous solutions consisting of mixtures of [C12mpip][AcSa] and sodium salicylate (SS), an hydrotope additive, were carried out. The analysis of zero shear viscosity and moduli properties as a function of concentration and temperature reveals that the addition of SS promotes the growth of small ellipsoid aggregates into large worm-like structures with a typical viscoelastic gel behavior. The moduli properties vs temperature profiles are complex and no hysteresis was produced in heating and cooling modes, suggesting the thermoirreversibile and complex nature

  5. Detection of Salicylic Acid in Willow Bark: An Addition to a Classic Series of Experiments in the Introductory Organic Chemistry Laboratory

    Science.gov (United States)

    Clay, Matthew D.; McLeod, Eric J.

    2012-01-01

    Salicylic acid and its derivative, acetylsalicylic acid, are often encountered in introductory organic chemistry experiments, and mention is often made that salicylic acid was originally isolated from the bark of the willow tree. This biological connection, however, is typically not further pursued, leaving students with an impression that biology…

  6. MDR1 is Related to Intestinal Epithelial Injury Induced by Acetylsalicylic Acid

    Directory of Open Access Journals (Sweden)

    Munehiro Kugai

    2013-10-01

    Full Text Available Background/Aims: Although the cytotoxicity of aspirin against the intestinal epithelium is a major clinical problem, little is known about its pathogenesis. We assessed the involvement of Multi Drug Resistance (MDR 1 in intestinal epithelial cell injury caused by aspirin using MDR1 gene-transfected Caco2 cells. Methods: Caco2 cells were treated with various concentrations of aspirin for 24 h. After treatment of Caco2 cells with verapamil, a specific inhibitor of MDR1, we assessed the extent of cell injury using a WST-8 assay at 24 h after aspirin-stimulation. We performed the same procedure in MDR1 gene-transfected Caco2 cells. To determine the function of MDR1 in the metabolism of aspirin, flux study was performed using 14C-labeled aspirin. Results: The level of aspirin-induced cell injury was higher in verapamil-treated Caco2 cells than in control cells and was less serious in MDR1-transfected Caco2 cells than in control vector-transfected cells. The efflux of 14C-labeled aspirin was higher in verapamil-treated Caco2 cells than in control cells. Conclusion: These data suggest that aspirin effux occurs through the MDR1 transporter and that the MDR1 transporter is involved in the pathogenesis of aspirin-induced cell injury.

  7. Chemoprevention with Acetylsalicylic Acid, Vitamin D and Calcium Reduces Risk of Carcinogen-induced Lung Tumors

    DEFF Research Database (Denmark)

    Pommergaard, Hans-Christian; Burcharth, Jakob; Rosenberg, J

    2013-01-01

    Background/Aim: Research has shown that chemoprevention may be effective against the development of lung cancer. The purpose of the present study was to evaluate the effect of oral chemoprevention in a mouse model of tobacco carcinogen-induced lung tumor....

  8. Paracetamol (acetaminophen), aspirin (acetylsalicylic acid) and indomethacin are anti-androgenic in the rat foetal testis

    DEFF Research Database (Denmark)

    Kristensen, David Møbjerg; Lesné, L.; Fol, V. Le

    2012-01-01

    More than half the pregnant women in the Western world report taking mild analgesics. These pharmaceutical compounds have been associated with congenital cryptorchidism in humans, the best-known risk factor for low semen quality and testicular germ cell cancer. Furthermore, some of these mild ana...

  9. The combination of 1α, 25(OH)2 – Vitamin D3, calcium and acetylsalicyclic acid affects azoxymethane-induced aberrant crypt foci and colorectal tumours in rats

    DEFF Research Database (Denmark)

    Mølck, Anne-Marie; Poulsen, Morten; Meyer, Otto A.

    2002-01-01

    Effects of 1alpha,25(OH)(2)-vitamin D(3) and acetylsalicylic acid at various dietary levels of calcium (CaCO(3)) on development of aberrant crypt foci (ACF) and tumours in colon were examined in groups of 16 male F344 rats initiated with azoxymethane and observed for 16 weeks. Calcium was the most...... potent modulator of ACF development. The total number of ACF increased with low calcium and decreased with high calcium. The number of large ACF decreased with any addition of calcium, acetylsalicylic acid and 1alpha,25(OH)(2)-vitamin D(3). High levels of calcium alone or in combination with 1alpha,25(OH......)(2)-vitamin D(3) increased the incidence of tumour-bearing animals. 1alpha,25(OH)(2)-vitamin D(3) and acetylsalicylic acid at 5,000 ppm calcium increased the incidence as well....

  10. Synthesis of [{sup 11}C]salicylic acid and related compounds and their biodistribution in mice

    Energy Technology Data Exchange (ETDEWEB)

    Sasaki, Toru; Ishii, Shin-Ichi; Senda, Michio [Positron Medical Center, Tokyo Metropolitan Institute of Gerontology, Nakacho, Itabashi, Tokyo (Japan); Ogawa, Koji [Radiological Technology Course, Faculty of Medical Engineering and Technology, School of Allied Health Sciences, Kitasato University, Kanagawa (Japan)

    1999-05-01

    For in vivo measurement of the hydroxyl radical ({sup %s{center_dot}}OH), we synthesized [{sup 11}C]salicylic acid, [{sup 11}C]O-acetylsalicylic acid and [{sup 11}C]2-methoxybenzoic acid by carboxylation of 2-bromomagnesiumanisol using [{sup 11}C]CO{sub 2}. The radiochemical yield of [{sup 11}C]salicylic acid, [{sup 11}C]O-acetylsalicylic acid and [{sup 11}C]2-methoxybenzoic acid calculated from trapped [{sup 11}C]CO{sub 2} in a liquid argon cooled stainless tube was 7.3{+-}1.6, 5.2 and 10.2{+-}1.7% (decay corrected), respectively. The uptake of {sup 11}C tracers by mouse brain was 0.46, 0.32 and 0.46% dose/g tissue, respectively, at 10 min post injection and presented washout patterns thereafter.

  11. An effective antidote for paraquat poisonings: the treatment with lysine acetylsalicylate.

    Science.gov (United States)

    Dinis-Oliveira, R J; Pontes, H; Bastos, M L; Remião, F; Duarte, J A; Carvalho, F

    2009-01-31

    Sodium salicylate (NaSAL) has been shown to have a multifactorial protection mechanism against paraquat (PQ)-induced toxicity, due to its ability to modulate inflammatory signalling systems, to prevent oxidative stress and to its capacity to chelate PQ. Considering that currently there is no pharmaceutical formulation available for parenteral administration of NaSAL, the aim of the present study was to evaluate the antidotal feasibility of a salicylate prodrug, lysine acetylsalicylate (LAS), accessible for parenteral administrations. PQ was administered to Wistar rats by gavage (125mg/kg of PQ ion) and the treatment was performed intraperitoneally with different doses (100, 200 and 400mg/kg of body weight) of LAS. Survival rate was followed during 30 days and living animals at this endpoint were sacrificed for lung, kidney, liver, jejune and heart histological analysis. It was shown, that the salicylate prodrug, LAS, available in a large number of hospitals, is also effective in the treatment of PQ intoxications. From all tested LAS doses, 200mg/kg assured animal's full survival. Comparatively to 60% of mortality observed in PQ only exposed animals, the lethality was higher (80%) in the group that received 400mg/kg of LAS 2h after PQ administration. The dose of 100mg/kg of LAS showed only a modest protection (60% of survival). Collagen deposition was observed by histological analysis in survived animals of all experimental groups, being less pronounced in animals receiving 200mg/kg of LAS, reinforcing the importance of this dose against tissue damage induced by PQ. The results allow us to suggest that LAS should be considered in the hospital treatment of PQ poisonings.

  12. Lysine acetylsalicylate ameliorates lung injury in rats acutely exposed to paraquat

    Institute of Scientific and Technical Information of China (English)

    HUANG Wei-dong; WANG Jie-zan; LU Yuan-qiang; DI Ya-min; JIANG Jiu-kun; ZHANG Qin

    2011-01-01

    Background Paraquat (PQ), an effective and widely used herbicide, has been proven to be safe when appropriately applied to eliminate weeds. However, PQ poisoning is an extremely frustrating clinical condition with a high mortality and with a lack of effective treatments in humans. PQ mainly accumulates in the lung, and the main molecular mechanism of PQ toxicity is based on redox cycling and intracellular oxidative stress generation. The aim of this study was to evaluate whether lysine acetylsalicylate (LAS) could protect the lung from the damage of PQ poisoning and to study the mechanisms of protection.Methods A model of PQ poisoning was established in 75 Sprague-Dawley rats by intragastric administration of 50 mg/kg PQ, followed by treatment with 200 mg/kg of LAS. The rats were randomly divided into sham, PQ, and PQ+LAS groups, with 25 in each group. We assessed and compared the malonaldehyde (MDA) content, superoxide dismutase activity (SOD), glutathion peroxidase (GSH-Px), and catalase (CAT) in serum and lung and the hydroxyproline (HYP)content, pathological changes, apoptosis and expression of Bcl-2/Bax protein in lung of rats on days 1, 3, 7, 14 and 21after PQ poisoning and LAS treatment.Results Compared to the PQ group rats, early treatment with LAS reduced the MDA and HYP contents, and increased the SOD, GSH-Px, and CAT activities in the serum and lung on days 1, 3, 7, 14, and 21 after PQ poisoning (all P<0.05).After early LAS treatment, the apoptotic rate and Bax expression of lung decreased, the Bcl-2 expression increased, and the Bcl-2/Bax ratio increased, compared to the PQ group rats. Furthermore, the pathological results of lungs revealed that after LAS treatment, early manifestations of PQ poisoning, such as hemorrhage, edema and inflammatory-cell infiltration, were improved to some degree, and collagen fibers in the pulmonary interstitium were also obviously reduced.Conclusion In this rat model of PQ poisoning, LAS effectively ameliorated the lung

  13. Lysine acetylsalicylate increases the safety of a paraquat formulation to freshwater primary producers: A case study with the microalga Chlorella vulgaris

    Energy Technology Data Exchange (ETDEWEB)

    Baltazar, Maria Teresa, E-mail: mteresabaltazar@gmail.com [REQUIMTE, Laboratory of Toxicology, Department of Biological Sciences, Faculty of Pharmacy, University of Porto, Rua Jorge Viterbo Ferreira, 228, 4050-313 Porto (Portugal); IINFACTS-Institute of Research and Advanced Training in Health Sciences and Technologies, Department of Sciences, Advanced Institute of Health Sciences-North, CESPU, CRL, Rua Central de Gandra, 1317, 4585-116 Gandra (Portugal); Dinis-Oliveira, Ricardo Jorge [REQUIMTE, Laboratory of Toxicology, Department of Biological Sciences, Faculty of Pharmacy, University of Porto, Rua Jorge Viterbo Ferreira, 228, 4050-313 Porto (Portugal); IINFACTS-Institute of Research and Advanced Training in Health Sciences and Technologies, Department of Sciences, Advanced Institute of Health Sciences-North, CESPU, CRL, Rua Central de Gandra, 1317, 4585-116 Gandra (Portugal); Department of Legal Medicine and Forensic Sciences, Faculty of Medicine, University of Porto, Alameda Professor Hernâni Monteiro, 4200-319 Porto (Portugal); CENCIFOR-Forensic Sciences Center, Largo da Sé Nova, 3000-213, Coimbra (Portugal); Martins, Alexandra [CIIMAR Interdisciplinary Centre of Marine and Environmental Research, Laboratory of Ecotoxicology and Ecology, Rua dos Bragas, 289, 4050-123 Porto (Portugal); ICBAS-Institute of Biomedical Sciences of Abel Salazar, University of Porto, Department of Populations Studies, Laboratory of Ecotoxicology, Rua Jorge Viterbo Ferreira, 228, 4050-313 Porto (Portugal); Bastos, Maria de Lourdes [REQUIMTE, Laboratory of Toxicology, Department of Biological Sciences, Faculty of Pharmacy, University of Porto, Rua Jorge Viterbo Ferreira, 228, 4050-313 Porto (Portugal); Duarte, José Alberto [CIAFEL, Faculty of Sports, University of Porto, Rua Dr. Plácido Costa, 91-4200-450 Porto (Portugal); and others

    2014-01-15

    Highlights: •The formulation has a reduced toxicity to C. vulgaris when compared to Gramoxone{sup ®}. •The highest protection was achieved at the proportion of 1:8 (PQ/LAS). •LAS conferred a protection of approximately 1.8 fold (% of inhibition of growth). •Salicylic acid is biotransformed by C. vulgaris after 48 h, and not detectable at 96 h. -- Abstract: Large amounts of herbicides are presently used in the industrialized nations worldwide, with an inexorable burden to the environment, especially to aquatic ecosystems. Primary producers such as microalgae are of especial concern because they are vital for the input of energy into the ecosystem and for the maintenance of oxygen in water on which most of other marine life forms depend on. The herbicide paraquat (PQ) is known to cause inhibition of photosynthesis and irreversible damage to photosynthetic organisms through generation of reactive oxygen species in a light-dependent manner. Previous studies have led to the development of a new formulation of PQ containing lysine acetylsalicylate (LAS) as an antidote, which was shown to prevent the mammalian toxicity of PQ, while maintaining the herbicidal effect. However, the safety of this formulation to primary producers in relation to commercially available PQ formulations has hitherto not been established. Therefore, the aim of this study was to evaluate the toxicity of the PQ + LAS formulation in comparison with the PQ, using Chlorella vulgaris as a test organism. Effect criterion was the inhibition of microalgal population growth. Following a 96 h exposure to increasing concentrations of PQ, C. vulgaris growth was almost completely inhibited, an effect that was significantly prevented by LAS at the proportion used in the formulation (PQ + LAS) 1:2 (mol/mol), while the highest protection was achieved at the proportion of 1:8. In conclusion, the present work demonstrated that the new formulation with PQ + LAS has a reduced toxicity to C. vulgaris when

  14. [Effect of magnesium, acetylsalicilic acid and emoxypine on aggregation of platelets].

    Science.gov (United States)

    Loznikova, S Zh; Sukhodola, A A; Shcharbina, N Iu; Shcharbin, D G

    2014-01-01

    The thrombin-induced platelet aggregation was studied in the absence and presence of magnesium sulfate, acetylsalicylic acid and emoxypine. It was found that all the preparations studied were able separately to decrease platelet aggregation. In contrast, their joint action was not able to affect the aggregation of platelets. The data obtained can be used to choose the treatment strategy for patients with ischemic stroke.

  15. Short-term beneficial effect of aspirin in patient with chronic rhinosinusitis and tolerant to acetylsalicylic acid.

    Directory of Open Access Journals (Sweden)

    Ali Kutlu

    2013-12-01

    Full Text Available It is well known that desensitization treatment with aspirin can significantly improve symptoms and quality of life in patient with aspirin-exacerbated respiratory disease. However, its mechanism has not been clearly understood yet. In this case report, 41-year-old male patient was referred to our allergy and immunology department with complaints of chronic rhinosinusitis including postnasal discharge, sneezing, facial pain/pressure, waking up tired, nasal obstruction, smell loss for a long time. According to the patient, the complaints were controlled partially with nasal steroid and antihistamines, and single dose parenteral depot steroids were highly effective in controlling the symptoms and each time this effect lasted at least three weeks. The patient was told to use aspirin when needed analgesic and he started to use aspirin 500 mg bid. po for 10 days for his pain in the joints. The patient stressed the superiority of aspirin over other drugs including oral antihistamine and LTA and its equality to systemic steroid drugs in suppressing symptoms. It seemed that aspirin had positive effects in allergic inflammation at least in some subset of aspirin tolerant patients with chronic sinusitis.

  16. Improved Synthesis of Acetylsalicylic Acid%乙酰水杨酸合成方法改进

    Institute of Scientific and Technical Information of China (English)

    李远军; 陈丽

    2010-01-01

    以水杨酸和乙酸酐为原料,以弱酸硫酸铝钾作催化剂可以方便的合成乙酰水杨酸,实验结果表明:反应温度、反应时间、催化剂用量、水杨酸与乙酸酐的比例等因素均有影响,最佳反应条件是:催化剂的用量为0.6g,n(水杨酸):n(乙酸酐)=1.0:2.0,恒温70℃,反应时间为30min,在优化的反应条件下,乙酰水杨酸的产率为77.8%.结果还表明,硫酸铝钾作为催化剂产率高于浓硫酸作催化剂的产率,而且产品色泽为白色,且纯度高.

  17. 碘催化合成乙酰水杨酸%Synthesis of Acetylsalicylic Acid with Iodine as Catalyst

    Institute of Scientific and Technical Information of China (English)

    原方圆; 邵红兵; 董丽花

    2008-01-01

    乙酰水杨酸(2-乙酰氧基苯甲酸)俗称阿司匹林,是一种常用的解热镇痛药,作为治疗和预防心脑血管疾病的药物已被广泛应用于临床。近年来的研究表明:阿司匹林能有效防治动脉梗塞,抑制血小板聚集,在防治心血管疾病方面有较好的疗效,服用阿司匹林能使胆道再次结石的可能性减少50%,使人患自内障的可能性减少70%,对防治乳腺癌、肺癌、皮肤癌也有较好的功效。乙酰水杨酸(阿司匹林)通常用水杨酸和乙酸酐反应来合成,

  18. Synthesis of acetylsalicylic acid catalyzed by urea%尿素催化合成乙酰水杨酸

    Institute of Scientific and Technical Information of China (English)

    郑广进; 龙盛京

    2010-01-01

    以水杨酸和乙酸酐为原料,采用尿素作催化剂合成乙酰水杨酸.考察了温度、尿素用量、n(水杨酸):n(乙酸酐)和时间对反应的影响.正交试验结果表明,较适宜的反应条件为:n(水杨酸):n(乙酸酐)=1:3,尿素用量为水杨酸质量的5%,反应温度85℃,反应时间60 min,此条件下,乙酰水杨酸收率达94.06%.

  19. Low-Dose Acetylsalicylic Acid in Treating Patients With Stage I-III Non-Small Cell Lung Cancer

    Science.gov (United States)

    2016-06-28

    Adenocarcinoma of the Lung; Recurrent Non-small Cell Lung Cancer; Stage IA Non-small Cell Lung Cancer; Stage IB Non-small Cell Lung Cancer; Stage IIA Non-small Cell Lung Cancer; Stage IIB Non-small Cell Lung Cancer; Stage IIIA Non-small Cell Lung Cancer; Stage IIIB Non-small Cell Lung Cancer

  20. Separation of Aliphatic and Aromatic Carboxylic Acids by Conventional and Ultra High Performance Ion Exclusion Chromatography.

    Science.gov (United States)

    Mansour, Fotouh R; Kirkpatrick, Christine L; Danielson, Neil D

    2013-06-01

    An ion exclusion chromatography (IELC) comparison between a conventional ion exchange column and an ultra-high performance liquid chromatography (UHPLC) dynamically surfactant modified C18 column for the separation of an aliphatic carboxylic acid and two aromatic carboxylic acids is presented. Professional software is used to optimize the conventional IELC separation conditions for acetylsalicylic acid and the hydrolysis products: salicylic acid and acetic acid. Four different variables are simultaneously optimized including H2SO4 concentration, pH, flow rate, and sample injection volume. Thirty different runs are suggested by the software. The resolutions and the time of each run are calculated and feed back to the software to predict the optimum conditions. Derringer's desirability functions are used to evaluate the test conditions and those with the highest desirability value are utilized to separate acetylsalicylic acid, salicylic acid, and acetic acid. These conditions include using a 0.35 mM H2SO4 (pH 3.93) eluent at a flow rate of 1 mL min(-1) and an injection volume of 72 μL. To decrease the run time and improve the performance, a UHPLC C18 column is used after dynamic modification with sodium dodecyl sulfate. Using pure water as a mobile phase, a shorter analysis time and better resolution are achieved. In addition, the elution order is different from the IELC method which indicates the contribution of the reversed-phase mode to the separation mechanism.

  1. SYNTHESIS OF ACETYLSALICYLIC ACID CATALYZED BY SILICOTUNGSTIC ACID%硅钨酸催化合成乙酰水杨酸

    Institute of Scientific and Technical Information of China (English)

    徐常龙; 柳闽生; 曹小华; 赵新萍; 薛蒙伟

    2007-01-01

    以水杨酸和乙酸酐为原料,硅钨酸为催化剂合成了乙酰水杨酸.考察了催化剂用量、反应物物料配比、反应时间、温度等因素对反应的影响.结果表明:硅钨酸具有催化活性高、稳定,对环境友好的特点.最佳工艺条件为:n(水杨酸):n(乙酸酐):n(硅钨酸)=1.0:2.5:0.002 4,76~80 ℃反应15 min,乙酰水杨酸收率达92.6%.

  2. 酸性膨润土催化合成乙酰水杨酸研究%Studies on synthesis of acetylsalicylic acid catalyzed by acid bentonite

    Institute of Scientific and Technical Information of China (English)

    陈志勇; 何奕波

    2005-01-01

    以水杨酸和乙酸酐为原料,在自制酸性膨润土催化下合成了乙酰水杨酸;探讨了催化剂的结构特征及最佳合成条件.结果表明:酸性膨润土对乙酰水杨酸的合成具有良好催化活性;在水杨酸与乙酸酐投料比为1∶ 3.6,酸性膨润土加入量等于5%水杨酸投料量(质量)和85~90 ℃下,催化反应0.5~1.0 h,产物收率可达90.44%.

  3. 氨基磺酸催化合成乙酰水杨酸的研究%Synthesis of acetylsalicylic acid over sulfaminic acid supported on activated carbon

    Institute of Scientific and Technical Information of China (English)

    李继忠; 王俊梅; 田曼

    2008-01-01

    以水杨酸和乙酸酐为原料,采用氨基磺酸作催化剂合成乙酰水杨酸.考察了影响反应的因素.结果表明,酰化反应的优化条件为:n(水杨酸):n(乙酸酐):n(氨基磺酸)=1:1.5:0.006 1,反应时间25 min,反应温度(81~85)℃,产率可达93.34%.

  4. 以酸活化膨润土催化合成阿司匹林%Synthesis of acetylsalicylic acid by acid bentonite as catalyst

    Institute of Scientific and Technical Information of China (English)

    王贵全; 陈志勇

    2004-01-01

    以水杨酸和乙酸酐为原料,在自制酸化膨润土催化下合成了阿司匹林;探讨了催化剂的结构特征及最佳催化条件.结果表明:酸化膨润土对阿司匹林的合成具有良好的催化活性;在最佳工艺条件下,收率可达:90.44%.

  5. 负载型杂多酸催化合成乙酰水杨酸的研究%Synthesis of Acetylsalicylic Acid Catalyzed by Supported Heteropoly Acid

    Institute of Scientific and Technical Information of China (English)

    谢宝华; 曹小华; 徐常龙; 陶春元

    2007-01-01

    以水杨酸和乙酸酐为原料,负载型杂多酸为催化剂合成了乙酰水杨酸.考察催化剂用量、水杨酸和乙酸酐物料配比、反应时间、温度等因素对反应的影响.结果表明:当n(水杨酸)∶n(乙酸酐)为1.0∶1.5,催化剂用量为水杨酸质量的5%,71~75 ℃反应15 min,产率达94.2%.

  6. 氨基磺酸催化合成乙酰水杨酸的研究%Study on Synthesis of Acetylsalicylic Acid Catalyzed by Amidosulphonic Acid

    Institute of Scientific and Technical Information of China (English)

    杨树

    2007-01-01

    利用氨基磺酸作为催化剂,由水杨酸和乙酸酐合成了乙酰水杨酸.研究了各因素对该反应的影响.通过实验确定了其最佳反应条件.实验表明:该催化剂催化效果好,使用量少,产率高,三废排放少,廉价易得.

  7. Synthesis of a nano-crystalline solid acid catalyst from fly ash and its catalytic performance

    Energy Technology Data Exchange (ETDEWEB)

    Chitralekha Khatri; Ashu Rani [Government P.G. College, Kota (India). Environmental Chemistry Laboratory

    2008-10-15

    The synthesis of nano-crystalline activated fly ash catalyst (AFAC) with crystallite size of 12 nm was carried out by chemical and thermal treatment of fly ash, a waste material generated from coal-burning power plants. Fly ash was chemically activated using sulfuric acid followed by thermal activation at 600{sup o}C. The variation of surface and physico-chemical properties of the fly ash by activation methods resulted in improved acidity and therefore, catalytic activity for acid catalyzed reactions. The AFAC was characterized by X-ray diffraction, FT-IR spectroscopy, N{sub 2}-adsorption-desorption isotherm, scanning electron microscopy, flame atomic absorption spectrophotometry and sulfur content by CHNS/O elemental analysis. It showed amorphous nature due to high silica content (81%) and possessed high BET surface area (120 m{sup 2}/g). The catalyst was found to be highly active solid acid catalyst for liquid phase esterification of salicylic acid with acetic anhydride and methanol giving acetylsalicylic acid and methyl salicylate respectively. A maximum yield of 97% with high purity of acetylsalicylic acid (aspirin) and a very high conversion 87% of salicylic acid to methyl salicylate (oil of wintergreen) was obtained with AFAC. The surface acidity and therefore, catalytic activity in AFAC was originated by increased silica content, hydroxyl content and higher surface area as compared to fly ash. The study shows that coal generated fly ash can be converted into potential solid acid catalyst for acid catalyzed reactions. Furthermore, this catalyst may replace conventional environmentally hazardous homogeneous liquid acids making an ecofriendly; solvent free, atom efficient, solid acid based catalytic process. 27 refs., 5 figs., 2 tabs.

  8. The Effects of Salicylic Acid on Juvenile Zebrafish Danio rerio Under Flow-Through Conditions.

    Science.gov (United States)

    Zivna, Dana; Blahova, Jana; Siroka, Zuzana; Plhalova, Lucie; Marsalek, Petr; Doubkova, Veronika; Zelinska, Gabriela; Vecerek, Vladimir; Tichy, Frantisek; Sehonova, Pavla; Svobodova, Zdenka

    2016-09-01

    The aquatic environment is becoming increasingly contaminated with pharmaceuticals. Salicylic acid (SA), which can be used individually or appear as a degradation product of the widely used acetylsalicylic acid was chosen for testing. Juvenile zebrafish Danio rerio were subjected to OECD test No. 215 (fish, juvenile growth test) with salicylic acid concentrations of 0.004; 0.04; 0.4; 4 and 40 mg/L. Specific growth rate (SGR), histological changes, and parameters of oxidative stress were evaluated. SA had no effects on histological changes, SGR, glutathione reductase, and lipid peroxidation. Increased catalytic activity of GPx was found at 0.04 mg/L compared to control, increased catalytic activity of catalase was found at 0.04 and 4 mg/L compared to control, and increased catalytic activity of glutathione-S-transferase was found at 0.004 and 0.04 mg/L compared to control (P salicylic acid.

  9. Exantema hemorrágico por virus dengue inducido por ácido acetil-salicílico Haemorrhagic exanthema due to dengue virus induced by acetylsalicylic acid

    OpenAIRE

    Valerio, L.; X. de Balanzó; Jiménez, O.; M. L. Pedro-Botet

    2006-01-01

    El dengue, enfermedad infecciosa vírica propia de los climas tropicales, se considera una patología reemergente que ha dado lugar a graves epidemias en la última década. En la expansión del virus y de su mosquito vector se barajan factores relacionados con la alteración humana del medio, con la rapidez en el tránsito de mercancias y personas y debidos al cambio climático. Como reflejo de ello, se asiste a un aumento de casos importados que, al ser una enfermedad con periodo de incubación cort...

  10. Study of the teratogenicity of acetylsalicylic acid in SD rats%阿司匹林对SD大鼠致畸作用的研究

    Institute of Scientific and Technical Information of China (English)

    赵敏; 陈壁锋; 杨杏芬; 周轶琳; 黄俊明; 谭剑斌; 陈瑞仪

    2009-01-01

    目的 评价阿司匹林对SD大鼠的母体及胎仔毒性.方法 将32只SD孕鼠随机分为2个组(每组16只):阿司匹林组(280 mg/kg)及对照组,阿司匹林组大鼠于受孕的第7~16天灌胃给予阿斯匹林(溶剂为1.5%羧甲基纤维素钠),对照组给予1.5%羧甲基纤维素钠,灌胃量均为每天1.0 mL/100g·BW.受孕的0、7、12、16、20d称量体重,在妊娠的第20天,颈椎脱臼处死,计数活胎数、死胎数和吸收胎数;观察胎仔外观、称量其体重后,将每窝1/2的活胎仔乙醇固定、氢氧化钾消化、茜素红染色、甘油透明后检查骨骼发育情况.另1/2活胎仔经Bouin's液固定后,检查内脏发育情况.结果 受试后阿司匹林组SD大鼠体重下降,16 d和20 d孕鼠体重及终期体重增重与对照组比较,差异均有统计学意义(P<0.01);阿司匹林组SD大鼠平均活胎数减少,吸收胎数及死胎数增加,活胎平均体重降低,身长和尾长缩短,各指标与对照组比较,差异均有统计学意义(P<0.01);外观畸形率、骨骼和内脏畸形率明显增加,与对照组比较,差异有统计学意义(P<0.05).结论 该实验条件下阿司匹林(280 mg/kg)对SD大鼠可能有明显的母体毒性和胚胎的致畸毒性.

  11. Synthesis of acetylsalicylic acid by microwave irradiation under the assistance of sodium bicarbonate catalyst%微波辐射催化合成乙酰水杨酸

    Institute of Scientific and Technical Information of China (English)

    李西安; 李丕高; 贺宝宝; 李苗

    2005-01-01

    在微波辐射下以碳酸氢钠为催化剂合成乙酰水杨酸,考察了影响反应的主要因素,实验结果表明合成最佳工艺条件为n(水杨酸):n(乙酸酐)=1:2.0,微波功率为微波炉"中低"档(40%)151 W,辐射时间45 s,催化剂用量为水杨酸质量的2%,产率可达96.9%(重结晶产率可达92.1%).

  12. Clear Synthesis of Acetylsalicylic Acid catalyzed by GY Zeoite%脱铝改性Y分子筛催化清洁合成乙酰水杨酸

    Institute of Scientific and Technical Information of China (English)

    张康华; 徐庆荣; 曹小华; 陈义凡; 陶春元

    2009-01-01

    以水杨酸和乙酸酐为原料,脱铝改性分子筛为催化剂合成了乙酰水杨酸.考察催化剂用量、水杨酸和乙酸酐物料配比、反应时间、反应温度等因素对该反应的影响.结果表明:当n(水杨酸):n(乙酸酐)为1.0:1.2,催化剂用量为水杨酸质量的7.5%,80 ℃,反应10 min,产物收率达94.2%.

  13. Synthesis of bis-cellobiose and bis-glucose derivatives of azacrown macrocycles as hosts in complexes with acetylsalicylic acid and 4-acetamidophenol.

    Science.gov (United States)

    Pintal, Michalina; Kryczka, Bogusław; Marsura, Alain; Porwański, Stanisław

    2014-03-11

    Two new C2 symmetric bis-cellobiose and bis-glucose azacrown derivatives were prepared according to the one-step procedure using azacrown ethers and azidosaccharides. Their complexes with aspirin and paracetamol were studied with the use of proton NMR spectroscopy. It was found that these pseudocryptands bind aspirin and paracetamol but each one in a different manner.

  14. Synthesis of Acetylsalicylic Acid under Microwave Radiation Condition by Vitamin C%维生素C催化微波合成乙酰水杨酸

    Institute of Scientific and Technical Information of China (English)

    郝红英; 周芳; 张强; 李海玲; 张莎莎

    2013-01-01

    以水杨酸和乙酸酐为原料,采用维生素C作催化剂微波辐射合成乙酰水杨酸.考察了催化剂用量、微波功率、辐射时间对反应产率的影响.优选出的较佳反应条件为:水杨酸6.3 g和新蒸馏乙酸酐9mL时,用维生素C0.5 g的催化剂,在400W的功率下催化40 s.在此条件下,乙酰水杨酸产率达60.60%.

  15. Hospital physicians' influence on gastrointestinal protection during treatment with non-steroidal anti-inflammatory drugs and acetylsalicylic acid and the impact on prescribing in primary care.

    Directory of Open Access Journals (Sweden)

    Michael Due Larsen

    Full Text Available BACKGROUND: The aim of this study was to describe the use of gastrointestinal (GI protection before, during and after hospitalisation for elderly patients using NSAID or low-dose ASA. METHODS: This study included all elderly patients (75+ admitted to hospital in the period of 1(st April 2010 to 31(st March 2011 at Odense University Hospital, Denmark, who were regular users of NSAID or low-dose ASA before hospital admission, or had one of these drugs initiated during hospital stay. By using pharmacy dispensing data and a hospital-based pharmacoepidemiological database, the treatment strategy for the individual patients was followed across hospital stay. RESULTS: In total, 3,587 patients were included. Before hospital admission, 93 of 245 NSAID users (38.0% and 597 of 1994 user of low-dose ASA (29.9% had used GI protection. During hospital stay, use of GI protection increased to 75% and 33.9%, respectively. When hospital physicians initiated new treatment with NSAID or with low-dose ASA, 305 of 555 (55.0% and 647 of 961 (67.3% were initiated without concomitant use of GI protection. When hospital physicians initiated GI protection, 26.8-51.0% were continued in primary care after discharge. CONCLUSIONS: During hospital stay, the use of GI protection increases, but when new treatment with NSAIDs or low-dose ASA is initiated in hospital, the use of gastrointestinal protection is low. The low use of GI protection is carried on in primary care after discharge.

  16. 复方乙酰水杨酸片的含量测定方法研究进展%Content Determination Methods for Compound Acetylsalicylic Acid Tablets

    Institute of Scientific and Technical Information of China (English)

    陆静; 李锐; 吕颖; 张海涛

    2009-01-01

    主要从实验条件方面综述了目前测定复方乙酰水杨酸片含量的几种方法.较为常用的有紫外分光光度法,FIA法,胶束薄层色谱法,单纯形加速法,高效液相色谱法等,这些方法稳定可信,测定结果准确可靠.

  17. Synthesis of Acetylsalicylic Acid with Microwave Radiation%微波辐射快速合成乙酰水杨酸

    Institute of Scientific and Technical Information of China (English)

    钟国清

    2003-01-01

    以水杨酸和乙酸酐为原料、无水碳酸钠作催化剂微波辐射快速合成乙酰水杨酸,并用正交试验筛选出最佳合成工艺条件:n(水杨酸)∶n(乙酸酐)=1∶2.0,微波功率464W,辐射时间60s,催化剂用量为水杨酸质量的2%,重结晶后产率可达90.8%.

  18. Compound Aspirin Tablets Acetylsalicylic Acid Determination%复方阿斯匹林片中乙酰水杨酸含量的测定

    Institute of Scientific and Technical Information of China (English)

    闫桂甫; 徐慧琴

    2010-01-01

    利用两步酸碱滴定法测定复方阿斯匹林片中乙酰水杨酸的含量,具有仪器简单、操作方便、结果准确度高等优点而被广泛采用:通过对市售几种标示量的复方阿斯匹林片的测定,及与国家药典规定相比较,结果满意.

  19. Improvement on the Synthetic Conditions of Acetylsalicylic Acid in Teaching Experiment%乙酰水杨酸合成条件的改进

    Institute of Scientific and Technical Information of China (English)

    王福生; 古昆; 曹槐

    2003-01-01

    利用正交试验设计对乙酰水杨酸合成实验的反应条件进行优化.结果表明,用2g水杨酸和4.2ml乙酸酐(1∶3,mol/mol)反应,固定催化剂浓硫酸的量0.1ml,在75℃下恒温反应12min是该合成反应的实验室最佳工艺条件.用该条件合成乙酰水杨酸,反应的稳定性好.

  20. 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.

  1. Synthesis of Acetylsalicylic Acid Catalyzed by Acetocaustin%三氯乙酸催化合成乙酰水杨酸

    Institute of Scientific and Technical Information of China (English)

    秦开成

    2013-01-01

    以水杨酸、乙酸酐为原料,三氯乙酸为催化剂合成乙酰水杨酸,探讨影响乙酰水杨酸的收率因素.实验结果显示:在催化剂用量为0.2 g,原料物质的量比为1∶1.5,反应温度为76~80℃,反应时间为5 min的条件下反应,其收率最高达78.97%.

  2. Investigation of primary nucleation phenomena of acetylsalicylic acid crystals induced by ultrasonic irradiation—ultrasonic energy needed to activate primary nucleation

    Science.gov (United States)

    Miyasaka, Etsuko; Ebihara, Satomi; Hirasawa, Izumi

    2006-09-01

    The purpose of our study is to clarify ultrasonic primary nucleation phenomena for controlling final product size by adjusting the number of primary nuclei. In our previous study, the effect of ultrasonic irradiation on the number of nuclei was investigated under the same supersaturated condition, as a result two novel phenomena were observed. First, there is a region where ultrasonic irradiation inhibits primary nucleation. Second, a specific amount of energy is needed to activate primary nucleation. From this result, it was expected that the ultrasonic energy needed to activate primary nucleation has a certain relationship to the energy necessary to form a stable nucleus. Therefore, we investigated the following: whether ultrasonic irradiation inhibits and activates primary nucleation at various degrees of supersaturation, whether final crystal size relates to the number of nuclei, and whether the ultrasonic energy needed to activate primary nucleation relates to the energy necessary to form a stable nucleus. First, we found that ultrasonic irradiation inhibits and activates primary nucleation at various supersaturated degrees. Second, we found that final crystal size increases or decreases depending on the number of nuclei. Therefore, it was indicated that ultrasonic energy could yield the desired crystal size by inducing suitable nucleation. Third, we found that the ultrasonic energy needed to activate primary nucleation decreases with a decrease in the energy necessary to form a stable nucleus. From this, we can propose criteria for determining the effect of ultrasonic irradiation on primary nucleation by showing diagrams correlating Δ Gcrit with Ecrit.

  3. Uptake of ascorbic acid by freshly isolated cells and secretory granules from the intermediate lobe of ox hypophyses

    DEFF Research Database (Denmark)

    Zhou, A; Matsumoto, T; Farver, O

    1990-01-01

    of uptake occurred when mechanically isolated cells were incubated with increasing ascorbic acid concentrations up to 0.6 mM. But if such cells were purified on a Percoll gradient, a clear saturation of uptake could be observed. Acetylsalicylic acid reduced the uptake markedly. When cells loaded with L-[14C......Mechanically isolated cells from the intermediate lobe of ox hypophyses contained 40.6 +/- 3.7 nmol mg-1 protein (mean +/- SE, n = 5) of ascorbic acid. They accumulated radioactivity time dependently, on incubation with L-[14C]ascorbic acid in ionic medium dominated by NaCl. No definite saturation......]ascorbic acid were homogenized and placed on a Percoll gradient, the radioactivity was recovered in several subcellular fractions. Decrease of the Na+ concentration or presence of ouabain in the medium did not cause noticeable changes in uptake by non-purified cells, whereas uptake by purified cells was clearly...

  4. Mechanism of Acetyl Salicylic Acid (Aspirin Degradation under Solar Light in Presence of a TiO2-Polymeric Film Photocatalyst

    Directory of Open Access Journals (Sweden)

    Debjani Mukherjee

    2016-04-01

    Full Text Available Application of titanium dioxide (TiO2 as a photocatalyst has presented a promising avenue for the safe photocatalytic degradation of pollutants. Increasing levels of the release of pharmaceuticals in the environment and formation of the intermediates during their degradation may impose health and environmental risks and therefore require more attention. Photocatalytic degradation of acetylsalicylic acid (aspirin was carried out in the presence of the TiO2-filled polymeric film as a photocatalyst under solar light irradiation. The polymeric film incorporates TiO2 in the matrix, which acts as a photocatalyst under solar illumination and degrades the acetyl salicylic acid (ASA into a range of organic compounds before complete demineralization (formation of carbon dioxide and water as final products. Among the intermediates, acetic acid was found to be present in a larger amount compared to other organic acids. The qualitative/quantitative analyses of the intermediates resulted in the determination of the most probable reaction’s mechanism in the degradation process. The mechanism of degradation of acetylsalicylic acid and its reaction pathway were developed from liquid chromatography/mass spectroscopy (LC/MS, Fourier Transform Infra Red (FTIR and UV spectrophotometric analysis. It was found that hydroxyl groups were dominant in the degradation process compared to electrons and holes generated by TiO2. The total organic carbon (TOC analysis was also carried out to analyze the organic carbon content of the intermediates formed during the course of degradation.

  5. Comparative studies about the influence of salicylic and acetylsalicilic acid on content of assimilatory pigments in the primary leaves of wheat (Triticum aestivum plantlets

    Directory of Open Access Journals (Sweden)

    Cornelia PURCAREA

    2007-05-01

    Full Text Available Salicylic acid (SA and some of its derivates are phenolic compounds recently recognized as plant growth regulators involved in many physiological processes including photosynthesis. One of the important derivates of Salicylic Acid is the Acetylsalicylic Acid. In the present investigation we studied the influence of exogenous Acetylsalicylic and Salicylic acid with different concentrations on the assimilatory pigments contents of the primary leaves of wheat seedlings in comparison with the same parameters of the control lots which were treated with water. The wheat seedlings were soaked for 6 hours in 0.01mM; 0.1mM; 0.5mM and 1 mM SA or ASA solutions and in water for the control lot, germinated for 7 days on filter paper moistened with water. After that, we planted the plantlets in sand and sprayed their coleoptiles and primary leaves, each day for an additional 7 days, with water. In the 14th days of germination we determined the content of assimilatory pigments extracted with N,N-dimethylformamide (DMF. The results showed that exogenous 0.01 mM, 0.1mM, 0.5 mM or 1.0 mM SA solution treatments cause more significant increases in the assimilatory pigments contents in leaves of wheat plantlets than treatments with ASA solutions of the same concentrations do.

  6. In vivo analgesic and anti-inflammatory activities of ursolic acid and oleanoic acid from Miconia albicans (Melastomataceae).

    Science.gov (United States)

    Vasconcelos, Maria Anita L; Royo, Vanessa A; Ferreira, Daniele S; Crotti, Antonio E Miller; Andrade e Silva, Márcio L; Carvalho, José Carlos T; Bastos, Jairo Kenupp; Cunha, Wilson R

    2006-01-01

    The aim of this work was to use in vivo models to evaluate the analgesic and anti-inflammatory activities of ursolic acid (UA) and oleanoic acid (OA), the major compounds isolated as an isomeric mixture from the crude methylene chloride extract of Miconia albicans aerial parts in an attempt to clarify if these compounds are responsible for the analgesic properties displayed by this plant. Ursolic acid inhibited abdominal constriction in a dose-dependent manner, and the result obtained at a content of 40 mg kg(-1) was similar to that produced by administration of acetylsalicylic acid at a content of 100 mg kg(-1). Both acids reduced the number of paw licks in the second phase of the formalin test, and both of them displayed a significant anti-inflammatory effect at a content of 40 mg kg(-1). It is noteworthy that the administration of the isolated mixture, containing 65% ursolic acid/35% oleanolic acid, did not display significant analgesic and anti-inflammatory activities. On the basis of the obtained results, considering that the mixture of UA and OA was poorly active, it is suggested that other compounds, rather than UA and OA, should be responsible for the evaluated activities in the crude extract, since the crude extract samples displayed good activities.

  7. Utilization of oriented crystal growth for screening of aromatic carboxylic acids cocrystallization with urea

    Science.gov (United States)

    Przybyłek, Maciej; Ziółkowska, Dorota; Kobierski, Mirosław; Mroczyńska, Karina; Cysewski, Piotr

    2016-01-01

    The possibility of molecular complex formation in the solid state of urea with benzoic acid analogues was measured directly on the crystallite films deposited on the glass surface using powder X-ray diffractometry (PXRD). Obtained solid mixtures were also analyzed using Fourier transform infrared spectroscopy (FTIR). The simple droplet evaporation method was found to be efficient, robust, fast and cost-preserving approach for first stage cocrystal screening. Additionally, the application of orientation effect to cocrystal screening simplifies the analysis due to damping of majority of diffraction signals coming from coformers. During validation phase the proposed approach successfully reproduced both positive cases of cocrystallization (urea:salicylic acid and urea:4-hydroxy benzoic acid) as well as pairs of co-formers immiscible in the solid state (urea:benzoic acid and urea:acetylsalicylic acids). Based on validated approach new cocrystals of urea were identified in complexes with 3-hydroxybenzoic acid, 2,4-dihydroxybenzoic acid, 2,5-dihydroxybenzoic acid, 2,6-dihydroxybenzoic acid and 3,5-dihydroxybenzoic acid. In all cases formation of multicomponent crystal phase was confirmed by the appearance of new reflexes on the diffraction patterns and FTIR absorption band shifts of O-H and N-H groups.

  8. Characterization of the binding sites for dicarboxylic acids on bovine serum albumin.

    Science.gov (United States)

    Tonsgard, J H; Meredith, S C

    1991-06-15

    Dicarboxylic acids are prominent features of several diseases, including Reye's syndrome and inborn errors of mitochondrial and peroxisomal fatty acid oxidation. Moreover, dicarboxylic acids are potentially toxic to cellular processes. Previous studies [Tonsgard, Mendelson & Meredith (1988) J. Clin. Invest. 82, 1567-1573] demonstrated that long-chain dicarboxylic acids have a single high-affinity binding site and between one and three lower-affinity sites on albumin. Medium-chain-length dicarboxylic acids have a single low-affinity site. We further characterized dicarboxylic acid binding to albumin in order to understand the potential effects of drugs and other ligands on dicarboxylic acid binding and toxicity. Progesterone and oleate competitively inhibit octadecanedioic acid binding to the single high-affinity site. Octanoate inhibits binding to the low-affinity sites. Dansylated probes for subdomain 2AB inhibit dodecanedioic acid binding whereas probes for subdomain 3AB do not. In contrast, low concentrations of octadecanedioic acid inhibit the binding of dansylated probes to subdomain 3AB and 2AB. L-Tryptophan, which binds in subdomain 3AB, inhibits hexadecanedioic acid binding but has no effect on dodecanedioic acid. Bilirubin and acetylsalicylic acid, which bind in subdomain 2AB, inhibit the binding of medium-chain and long-chain dicarboxylic acids. Our results suggest that long-chain dicarboxylic acids bind in subdomains 2C, 3AB and 2AB. The single low-affinity binding site for medium-chain dicarboxylic acids is in subdomain 2AB. These studies suggest that dicarboxylic acids are likely to be unbound in disease states and may be potentially toxic.

  9. Aspartic acid

    Science.gov (United States)

    Aspartic acid is a nonessential amino acids . Amino acids are building blocks of proteins. "Nonessential" means that our ... this amino acid from the food we eat. Aspartic acid is also called asparaginic acid. Aspartic acid helps ...

  10. 紫外二阶导数光谱法监测柠檬酸催化合成乙酰水杨酸%Monitoring synthesis systems of acetylsalicylic acid with citric acid as the catalyst by second derivative spectrometry

    Institute of Scientific and Technical Information of China (English)

    邵建群; 徐艳霞; 唐静成; 何深知; 张枫

    2015-01-01

    目的 采用紫外二阶导数光谱法监测柠檬酸催化合成乙酰水杨酸.方法 选择二阶导数光谱在289 nm和308 nm处的吸光度值,分别建立乙酰水杨酸和水杨酸质量浓度与二阶导数值的标准工作曲线.在不同温度条件下,实时监测合成反应体系中乙酰水杨酸和水杨酸的质量浓度.结果 反应温度为70℃、80℃、90 ℃和95℃,完成反应所需时间分别为80 min、50 min、20 min和15 min.结论 紫外二阶导数光谱法,可以实现对乙酰水杨酸合成过程的监测和判断反应终点.

  11. the Behaviour and Mechanism of Adsorption to Acetylsalicylic Acid by Acid and Alkali Modified Activated Carbon%酸碱改性活性炭吸附水中乙酰水杨酸的行为与机理

    Institute of Scientific and Technical Information of China (English)

    田颖霄; 王海芳; 卢静; 侯彬; 董慧科

    2016-01-01

    采用硝酸(HNO3)和氢氧化钠(NaOH)对活性炭表面进行改性,并考察其对乙酰水杨酸(ASP)的吸附性能.借助傅里叶红外光谱(FTIR)和扫描电镜(SEM)对改性活性炭结构特性进行表征,考察孔隙结构和官能团与吸附性能的关系,推断改性活性炭中对ASP起主要作用的官能团是含氧官能团.结果表明,两种改性活性炭对ASP均有良好的吸附效果;与Freundli-ch方程相比,吸附过程更适合用Langmuir方程来进行描述;也表明了活性炭对ASP的吸附属于单分子层吸附.改性后活性炭的最大吸附量可达到96.129 8 mg/g,且吸附过程更符合二级动力学方程.

  12. 对甲苯磺酸催化微波合成乙酰水杨酸的研究%Study on the microwave synthesis of acetylsalicylic acid by p-Toluene Sulphonic Acid catalyst

    Institute of Scientific and Technical Information of China (English)

    王立中; 卞小琴

    2008-01-01

    以水杨酸和乙酸酐为原料,以对甲苯磺酸为催化剂,微波辐射合成了乙酰水杨酸,并考察了影响反应的因素.实验表明:在n(水杨酸):n(乙酸酐)=1:1.7,催化剂用量为水杨酸质量的2.5%,微波输出功率为151W,辐射时间为60s,产率可达91.2%.

  13. HPLC法测定菊蓝抗流感片中乙酰水杨酸和游离水杨酸的含量%Determination of Acetylsalicylic acid and Salicylic Acid in Julan Anti-influenza Tablets by HPLC

    Institute of Scientific and Technical Information of China (English)

    袁晓芳; 张同波; 郝立芳

    2009-01-01

    目的:测定菊蓝抗流感片中乙酰水杨酸、水杨酸的含量.方法:采用HPLC法测定乙酰水杨酸、水杨酸的含量.色谱柱:Phenomenex C18柱,4.6mm×250mm,5μm流动相:乙腈-甲醇-0.01 mol·L-1磷酸二氢钾溶液-三乙胺(6:30:64:0.1,用磷酸调节pH值至3.3~3.4);检测波长:228 nm;柱温:35℃;进样量:20 μL.结果:乙酰水杨酸回归方程为Y=5.627×107X-2.042×105,r=0.999 9,线性范围为1.014 8~20.296μg,平均回收率为98.3%;水杨酸回归方程为Y=2.957×107X-5.442×104,r=0.999 9,线性范围为0.309 4~12.376μg.平均回收率为99.5%.结论:方法简便,快速,准确,为提高和完善该制剂的质量标准提供了依据.

  14. 对甲苯磺酸催化合成乙酰水杨酸的研究%Synthesis of Acetylsalicylic Acid with p-Toluene Sulphonic Acid Catalyst

    Institute of Scientific and Technical Information of China (English)

    李继忠

    2005-01-01

    以水杨酸和乙酸酐为原料,采用对甲苯磺酸作催化剂合成了乙酰水杨酸,考察了影响反应的因素.实验结果表明酰化反应的优化条件为水杨酸:乙酸酐:对甲苯磺酸摩尔比为1:2:0.0153,反应20 min,反应温度81~85℃,产率达94.44%.

  15. 对甲苯磺酸催化合成乙酰水杨酸的研究%Synthesis of Acetylsalicylic Acid with P—Toluene Sulphonic Acid Catalyst

    Institute of Scientific and Technical Information of China (English)

    冯艳辉; 王清斌

    2006-01-01

    以水杨酸和乙酸酐为原料,采用对甲苯磺酸作催化剂合成了乙酰水杨酸,采用正交实验法研究了影响反应的因素.实验结果表明酰化反应的优化条件为水杨酸:乙酸酐摩尔比为1:2,反应20 min,反应温度65~75℃.

  16. Aromatic hydroxylation of salicylic acid and aspirin by human cytochromes P450.

    Science.gov (United States)

    Bojić, Mirza; Sedgeman, Carl A; Nagy, Leslie D; Guengerich, F Peter

    2015-06-20

    Aspirin (acetylsalicylic acid) is a well-known and widely-used analgesic. It is rapidly deacetylated to salicylic acid, which forms two hippuric acids-salicyluric acid and gentisuric acid-and two glucuronides. The oxidation of aspirin and salicylic acid has been reported with human liver microsomes, but data on individual cytochromes P450 involved in oxidation is lacking. In this study we monitored oxidation of these compounds by human liver microsomes and cytochrome P450 (P450) using UPLC with fluorescence detection. Microsomal oxidation of salicylic acid was much faster than aspirin. The two oxidation products were 2,5-dihydroxybenzoic acid (gentisic acid, documented by its UV and mass spectrum) and 2,3-dihydroxybenzoic acid. Formation of neither product was inhibited by desferrioxamine, suggesting a lack of contribution of oxygen radicals under these conditions. Although more liphophilic, aspirin was oxidized less efficiently, primarily to the 2,5-dihydroxy product. Recombinant human P450s 2C8, 2C9, 2C19, 2D6, 2E1, and 3A4 all catalyzed the 5-hydroxylation of salicylic acid. Inhibitor studies with human liver microsomes indicated that all six of the previously mentioned P450s could contribute to both the 5- and 3-hydroxylation of salicylic acid and that P450s 2A6 and 2B6 have contributions to 5-hydroxylation. Inhibitor studies indicated that the major human P450 involved in both 3- and 5-hydroxylation of salicylic acid is P450 2E1.

  17. Salicylic acid induces apoptosis in colon carcinoma cells grown in-vitro: Influence of oxygen and salicylic acid concentration

    Energy Technology Data Exchange (ETDEWEB)

    Zitta, Karina; Meybohm, Patrick; Bein, Berthold; Huang, Ying; Heinrich, Christin; Scholz, Jens; Steinfath, Markus; Albrecht, Martin, E-mail: Albrecht@anaesthesie.uni-kiel.de

    2012-04-15

    In solid tumors the hypoxic environment can promote tumor progression and resistance to therapy. Recently, acetylsalicylic acid a major component of analgesic drugs and its metabolite salicylic acid (SA) have been shown to reduce the risk of colon cancer, but the mechanisms of action remain still unclear. Here we elucidate the effects of physiologically relevant concentrations of SA on colon carcinoma cells (CaCo-2) grown under normoxic and hypoxic conditions. Western blotting, caspase-3/7 apoptosis assays, MTS cell-proliferation assays, LDH cytotoxicity assays and hydrogen peroxide measurements were performed to investigate the effects of 1 and 10 {mu}M SA on CaCo-2 cells grown under normoxic conditions and cells exposed to hypoxia. Under normoxic conditions, SA did not influence cell proliferation or LDH release of CaCo-2 cells. However, caspase-3/7 activity was significantly increased. Under hypoxia, cell proliferation was reduced and LDH release and caspase-3/7 activities were increased. None of these parameters was altered by the addition of SA under hypoxic conditions. Hypoxia increased hydrogen peroxide concentrations 300-fold and SA significantly augmented the release of hydrogen peroxide under normoxic, but not under hypoxic conditions. Phosphorylation of the pro-survival kinases akt and erk1/2 was not changed by SA under hypoxic conditions, whereas under normoxia SA reduced phosphorylation of erk1/2 after 2 hours. We conclude that in colon carcinoma cells effects of SA on apoptosis and cellular signaling are dependent on the availability of oxygen. -- Highlights: Black-Right-Pointing-Pointer Effects of salicylic acid on colon carcinoma cells grown under normoxic and hypoxic conditions Black-Right-Pointing-Pointer Salicylic acid increases caspase-3/7 activity and hydrogen peroxide release under normoxia Black-Right-Pointing-Pointer Salicylic acid decreases pro-survival erk-1/2 phosphorylation under normoxia Black-Right-Pointing-Pointer Salicylic acid does

  18. Pharmaceutical salts and cocrystals involving amino acids: a brief structural overview of the state-of-art.

    Science.gov (United States)

    Tilborg, Anaëlle; Norberg, Bernadette; Wouters, Johan

    2014-03-03

    Salification of new drug substances in order to improve physico-chemical or solid-state properties (e.g. dissolution rate or solubility, appropriate workup process, storage for further industrial and marketing development) is a well-accepted procedure. Amino acids, like aspartic acid, lysine or arginine take a great part in this process and are implicated in several different formulations of therapeutic agent families, including antibiotics (amoxicillin from beta lactam class or cephalexin from cephalosporin class), NSAIDs (ketoprofen, ibuprofen and naproxen from profen family, acetylsalicylic acid) or antiarrhythmic agents (e.g. ajmaline). Even if more than a half of known pharmaceutical molecules possess a salifiable moiety, what can be done for new potential drug entity that cannot be improved by transformation into a salt? In this context, after a brief review of pharmaceutical salts on the market and the implication of amino acids in these formulations, we focus on the advantage of using amino acids even when the target compound is not salifiable by exploiting their zwitterionic potentialities for cocrystal edification. We summarize here a series of new examples coming from literature to support the advantages of broadening the application of amino acids in formulation for new drug substances improvement research for non-salifiable molecules.

  19. Comparison of antiplatelet regimens in secondary stroke prevention

    DEFF Research Database (Denmark)

    Christiansen, Christine Benn; Pallisgaard, Jannik; Gerds, Thomas Alexander

    2015-01-01

    BACKGROUND: In patients with ischemic stroke of non-cardioembolic origin, acetylsalicylic acid, clopidogrel, or a combination of acetylsalicylic acid and dipyridamole are recommended for the prevention of a recurrent stroke. The purpose of this study was to examine the risk of bleeding or recurrent...... were calculated for each antiplatelet regimen. RESULTS: Among patients discharged after first-time ischemic stroke, 3043 patients were treated with acetylsalicylic acid, 12,295 with a combination of acetylsalicylic acid and dipyridamole, and 3885 with clopidogrel. Adjusted HRs for clopidogrel versus...... the combination of acetylsalicylic acid and dipyridamole were 1.02 (95% confidence interval [CI]: 0.89-1.17) for ischemic stroke and 1.06 (95% CI: 0.83-1.35) for bleeding. Adjusted HRs for acetylsalicylic acid versus the combination of acetylsalicylic acid and dipyridamole were 1.48 (95% CI: 1.31-1.67) for stroke...

  20. In vitro ozone exposure increases release of arachidonic acid products from a human bronchial epithelial cell line

    Energy Technology Data Exchange (ETDEWEB)

    McKinnon, K.P.; Madden, M.C.; Noah, T.L.; Devlin, R.B. (TRC Environmental Corporation, Chapel Hill, NC (United States))

    1993-02-01

    Eicosanoids released after ozone exposure of a human bronchial epithelial cell line, BEAS-S6, were analyzed by high-pressure liquid chromatography (HPLC) of supernatants from exposed cells prelabeled with [3H]arachidonic acid. BEAS cells released thromboxane B2 (TxB2), prostaglandin E2 (PGE2), leukotriene C4 (LTC4), LTD4, LTE4, and 12-hydroxyheptadecatrienoic acid (HHT) after exposure to ozone at concentrations of 0.1, 0.25, 0.5, and 1.0 ppm. The eicosanoids were identified by coelution with authentic standards. The largest product from ozone-exposed BEAS cells was the most polar peak, designated Peak 1. Release of cyclooxygenase products such as TxB2, PGE2, and HHT was inhibited by acetylsalicylic acid. Peaks that migrated with authentic standards for LTB4, LTC4, and LTD4 were inhibited by the lipoxygenase inhibitor nordihydroguaiaretic acid. The leukotrienes LTB4 and LTC4/D4 could also be detected by immunoassay of concentrated peak fractions. Thus BEAS cells released eicosanoids from cyclooxygenase and lipoxygenase pathways of arachidonic acid metabolism following exposure to ozone. Airway epithelial cells may be an important source of eicosanoids following ozone stimulation in humans.

  1. Synthesis of Acetylsalicylic Acid under Microwave Radiation Using Sodium Bicarbonate as the Catalyst%NaHCO3催化微波合成乙酰水杨酸

    Institute of Scientific and Technical Information of China (English)

    郝红英; 吴建丽; 周芳; 李海玲; 张莎莎

    2013-01-01

    [目的]采用NaHCO3催化微波辐射法合成乙酰水杨酸.[方法]以水杨酸和乙酸酐为原料,碳酸氢钠作催化剂、采用微波辐射法合成乙酰水杨酸,通过单因素试验考察催化剂用量、微波功率、辐射时间对乙酰水杨酸产率的影响,并通过正交试验确定最佳工艺条件.[结果]优选出的最佳反应条件为:取6.3g水杨酸和9ml乙酸酐时,催化剂碳酸氢钠用量0.7g,微波辐射功率400W,辐射时间80 s.在此条件下,乙酰水杨酸产率达76.38%.[结论]该研究为乙酸水杨酸的合成提供了一种新的工艺.

  2. The Catalytic Synthesis of Acetylsalicylic Acid with Aluminium P-toluenesulfonate%对甲苯磺酸铝催化合成乙酰水杨酸的研究

    Institute of Scientific and Technical Information of China (English)

    蔡磊; 刘万毅

    2013-01-01

    经复分解反应制得了对甲苯磺酸铝,并用元素分析、IR、TGA等测试技术对产物的组成与结构进行了表针,并将其作为固体酸,用于催化水杨酸与乙酸酐合成乙酰水杨酸的O-酰化反应.实验结果表明,对甲苯磺酸铝对O-酰化反应表现出良好的催化活性,水杨酸与乙酸酐摩尔比1∶2(0.01 mol水杨酸),对甲苯磺酸铝0.15g,水浴温度75℃,反应时间35 min,乙酰水杨酸平均收率可达87%以上.

  3. Study on Synthesis of Acetylsalicylic Acid under Microwave Radiation Condition by Sodium Hydroxyethyl Sulfonate%羟乙基磺酸钠催化微波合成乙酰水杨酸的研究

    Institute of Scientific and Technical Information of China (English)

    郝红英; 尚磊; 陈超鹏

    2014-01-01

    以水杨酸和乙酸酐为原料,采用羟乙基磺酸钠作催化剂微波辐射合成乙酰水杨酸.考察了催化剂用量、微波功率、微波辐射时间对反应产率的影响.优选出的较佳反应条件为:取6.3g水杨酸和9mL乙酸酐时,催化剂羟乙基磺酸钠用量0.7 g,微波功率400W,微波辐射时间120 s.在此条件下,乙酰水杨酸产率达79.02%.

  4. 苯甲酸钠微波催化合成乙酰水杨酸的研究%Study on the Synthesis of Acetylsalicylic Acid with Sodium Benzoate by Microwave Radiation Method

    Institute of Scientific and Technical Information of China (English)

    郝红英; 侯巧芝; 肖培杰; 王慧星

    2014-01-01

    [目的]利用微波辐射法制备乙酰水杨酸.[方法]以水杨酸和乙酸酐为原料,以苯甲酸钠作为催化剂,微波辐射合成乙酰水杨酸.采用正交试验优化微波辐射苯甲酸钠催化合成乙酰水杨酸的工艺条件,并探讨合成工艺的影响因素.[结果]乙酰水杨酸的最佳合成工艺为:6.3 g水杨酸,9ml乙酸酐,催化剂苯甲酸钠用量0.4g,微波功率240W,辐射时间90s.在此优化条件下,乙酰水杨酸产率达67.07%.[结论]与传统合成工艺相比,微波辐射合成乙酰水杨酸反应时间短,产品收率高.

  5. Synthesis and Evaluation of Molecularly Imprinted Polymers Using Acetylsalicylic Acid as Template%乙酰水杨酸分子印迹聚合物的合成及性能研究

    Institute of Scientific and Technical Information of China (English)

    刘运美; 吕昌银; 范翔; 高治平

    2007-01-01

    采用分子印迹技术,以乙酰水杨酸为模板分子,1,4-二乙烯基苯为交联剂,分别以α-甲基丙烯酸和丙烯酰胺为功能单体,合成了对乙酰水杨酸具有特异性吸附能力的两种分子印迹聚合物;它们对乙酰水杨酸都存在两类不同亲和性的结合位点,其中用丙烯酰胺合成的分子印迹聚合物对模板分子乙酰水杨酸的氢键作用力和结合能力都比用α-甲基丙烯酸合成的聚合物强.这对分子印迹技术用于环境、血液等复杂样品中乙酰水杨酸的分离和富集具有重要意义.

  6. 微波辐射六氢吡啶催化快速合成乙酰水杨酸的研究%Research on rapid synthesis of acetylsalicylic acid catalysed by piperidine under microwave radiation

    Institute of Scientific and Technical Information of China (English)

    赵士举; 金秋; 苏惠; 李伟; 徐翠莲

    2010-01-01

    以水杨酸和乙酸酐为原料,微波辐射加热,六氢吡啶为催化剂,快速合成了乙酰水杨酸.通过正交试验及直观分析,探索出了最佳合成工艺条件;通过方差分析,得出了影响次序和程度.该方法为高效、环保、低能合成乙酰水杨酸提供了新的工艺条件.

  7. Na2CO3催化微波合成乙酰水杨酸的研究%Synthesis of Acetylsalicylic Acid under Microwave Radiation Condition by Sodium Carbonate

    Institute of Scientific and Technical Information of China (English)

    郝红英; 侯巧芝; 周芳; 张莎莎

    2013-01-01

    [目的]以水杨酸和乙酸酐为原料,采用碳酸钠作催化剂微波辐射合成乙酰水杨酸.[方法]采用正交试验法,考察了催化剂用量、微波功率、辐射时间对反应产率的影响.[结果]优选出的较佳反应条件为:取6.3g水杨酸和9ml乙酸酐,催化剂碳酸钠用量0.4g,微波功率400W,辐射时间90s.在此条件下,乙酰水杨酸产率达83.25%.[结论]采用碳酸钠微波催化合成乙酰水杨酸,反应收率较好.

  8. Synthesis and Biological Activities of the Conjugates of Acetylsalicylic Acid with Fungicide%乙酰水杨酸与杀菌剂的藕合物合成及生物活性

    Institute of Scientific and Technical Information of China (English)

    李俊凯; 徐汉虹; 谭堂峰; 朱建永

    2008-01-01

    通过乙酰水杨酸(ASA)分别与噻菌灵、三唑醇和(噁)鄂霉灵3种杀菌剂拼接,合成了未见文献报道的ASA-噻菌灵、ASA-三唑醇、ASA-(噁)霉灵的藕合物,并以未藕合的3种杀菌剂为对照,测定了3种藕合物对水稻纹枯病菌Rhizoctonia solani的室内毒力;以水杨酸(SA)为对照,测定了ASA-??霉灵藕合物对大豆叶片过氧化物酶(POD)活性的影响.结果表明,3种杀菌剂与ASA藕合后,杀菌毒力与藕合前的相当,同时还具有类似SA诱导植物POD活性升高的特性.

  9. Synthesis of Acetylsalicylic Acid Catalyzed by SiO24-/TiO2 Solid Superacid%SO24-/TiO2固体超强酸催化合成乙酰水杨酸

    Institute of Scientific and Technical Information of China (English)

    张晓丽; 任立国

    2008-01-01

    以水杨酸和乙酸酐为原料在SO24-/TiO2固体超强酸催化下合成了乙酰水杨酸.考察了催化剂的焙烧温度、反应时间、反应温度、原料配比、催化剂用量等对反应的影响以及催化荆的稳定性.确定最佳反应条件为:催化荆的焙烧温度500℃、反应温度90℃、反应时间40 min、n(乙酸酐):n(水杨酸)=2.0:1、催化剂用量1.0 g,此时乙酰水杨酸的收率可达77.8%.SO24-/TiO2固体超强酸催化荆制备简单、催化活性高、重复使用性好、后处理简便、无三废污染,符合节能环保的绿色催化发展趋势.

  10. Determination of Acetylsalicylic Acid in a spirit and pulsation capsules by HPLC%HPLC法测定行气脉动胶囊中乙酰水杨酸的含量

    Institute of Scientific and Technical Information of China (English)

    邢军; 李兰忠

    2005-01-01

    目的建立HPLC法测定行气脉动胶囊中乙酰水杨酸的含量.方法采用KromasilC18(250mm×4.6mm 5μm)柱,流动相为甲醇-0.1%二乙胺水溶液-冰醋酸(40:60:4),检测波长为280nm.结果测得线性范围为0.6~1.4mg·ml-1(r=0.9998),平均回收率为99.73%,RSD为1.23%(n=5).结论本法简便,准确.

  11. SYNTHESIS OF ACETYLSALICYLIC ACID CATALYZED BY SO42-/SILINAITE%固体超强酸SO42-/硅锂钠石催化合成乙酰水杨酸

    Institute of Scientific and Technical Information of China (English)

    刘达波; 邱祖民

    2008-01-01

    用浸渍法制备了SO42-/硅锂钠石固体超强酸催化剂,最佳工艺条件为:硫酸浸渍浓度0.25 mol/L,浸渍2 h,焙烧温度450℃,焙烧时同3 h.考察了催化剂用量、酸酐摩尔比及反应温度对乙酰水杨酸合成的影响,乙酰水扬酸的较佳制备工艺条件为:酸酐摩尔比1:2,催化剂的质量为水杨酸质量的1.5%,在75℃反应15min,乙酰水杨酸的收率达83.4%,催化剂可重复使用2次.

  12. Effect of 2.4-Dinitrophenol on acute toxicity of acetylsalicylic acid%2.4-二硝基酚对乙酰水杨酸急性毒性的影响

    Institute of Scientific and Technical Information of China (English)

    张富赓; 胡人杰; 姜卉

    2002-01-01

    目的:观察2.4-二硝基酚对乙酰水杨酸急性毒性的影响.方法:用简化机率法测定乙酰水杨酸与2.4-二硝基酚合用时小鼠的LD 50的影响.结果:乙酰水杨酸与2.4-二硝基酚合用时,其LD50约为文献记载的1/5.结论:2.4-二硝基酚可以增加乙酰水杨酸的毒性.

  13. 毛细管电泳法测定阿司匹林中乙酰水杨酸的含量%Determination of Acetylsalicylic Acid in Aspirin by Capillary Zone Electrophoresis

    Institute of Scientific and Technical Information of China (English)

    刘海兴; 刘凤芹; 于爱民; 孙效正; 李丽敏

    2006-01-01

    本文建立了毛细管电泳测定阿司匹林中乙酰水杨酸含量的新方法.确定的优化缓冲溶液是30 mmol/L硼砂溶液,pH为9.02.电泳电压为20 kV,紫外检测波长为214 nm.在此条件下水杨酸和乙酰水杨酸分离度较好,并测得了阿司匹林中乙酰水杨酸的含量.本法简便、快速.

  14. 超声辐射分子碘催化乙酰水杨酸的合成研究%Synthesis of Acetylsalicylic Acid Catalyzed by Molecular Iodine Under Ultrasound Irradiation

    Institute of Scientific and Technical Information of China (English)

    施小宁; 赵素瑞; 吴巧玲

    2008-01-01

    以碘作催化剂,以水杨酸和乙酸酐为原料,通过超声辐射快速合成了乙酰水杨酸.最佳合成条件为:原料比n(乙酸酐)∶n(水杨酸)∶n(碘)=100∶50∶1,超声功率300W,辐射时问15min,产率96.2%.研究结果表明该法反应时间短,操作简单,环境友好,节约能源,产率高.

  15. 微波辐射分子筛催化合成乙酰水杨酸的研究%Synthesis of Acetylsalicylic Acid by Microwave Irradiation with Molecular Sieve as Catalyst

    Institute of Scientific and Technical Information of China (English)

    刘鸿; 黄华

    2007-01-01

    介绍了一种采用微波辐射技术、分子筛催化合成乙酰水杨酸的方法,探讨了不同反应条件对产物收率的影响,实验结果表明:当n(水杨酸)∶n(乙酸酐)=1∶2.0、催化剂的用量为水杨酸质量的5%、微波辐射功率为200 W、辐射时间为2.5 min时,乙酰水杨酸的收率可达95.1%.

  16. Folic acid

    Science.gov (United States)

    ... taking folic acid by itself, or with L-carnitine a compound similar to an amino acid from ... levels. It is not clear if folic acid supplementation reduces hearing loss in people with normal folate ...

  17. Strong and long-lasting antinociceptive and anti-inflammatory conjugate of naturally occurring oleanolic acid and aspirin

    Directory of Open Access Journals (Sweden)

    Barbara Bednarczyk-Cwynar

    2016-07-01

    Full Text Available The conjugate 8 was obtained as a result of condensation of 3-hydroxyiminooleanolic acid morfolide (7 and aspirin in dioxane. Analgesic effect of OAO-ASA (8 for the range of doses 0.3 – 300.0 mg/kg (p.o. was performed in mice using a hot plate test. Anti-inflammatory activity was assessed on carrageenan-induced paw edema in rats for the same range of doses. The conjugate OAO-ASA (8 did not significantly change locomotor activity of mice, therefore sedative properties of the compound should be excluded. The compound 8 proved a simple, proportional, dose-dependent analgesic action and expressed strong anti-inflammatory activity showing a reversed U-shaped, dose-dependent relation with its maximum at 30.0 mg/kg. After its combined administration with morphine (MF, 5.0 mg/kg, s.c. the lowering of antinociceptive activity was found; however, the interaction with naloxone (NL, 3.0 mg/kg, s.c. did not affect the antinociceptive effect of OAO-ASA (8, therefore its opioid mechanism of action should be rather excluded. After combined administration with acetylsalicylic acid (ASA, 300.0 mg/kg, p.o. in hot-plate test, the examined compound 8 enhanced the antinociceptive activity in significant way. It also shows that rather the whole molecule is responsible for the antinociceptive and anti-inflammatory effect of the tested compound 8, however it cannot be excluded that the summarizing effect is produced by ASA released from the compound 8 and the rest of triterpene derivative. The occurrence of tolerance for triterpenic derivative 8 was not observed, since the analgesic and anti-inflammatory effects after chronic administration of the conjugate OAO-ASA (8 was on the same level as after its single treatment. It seemed that the anti-inflammatory mechanism of action of OAO-ASA (8 is not simple, even its chronic administration lowered both blood concentration of IL-6 and mRNA IL-6 expression. However, the effects of the conjugate OAO-ASA (8 on TNF-α level

  18. Acid-sensing ion channels expression, identity and role in the excitability of the cochlear afferent neurons

    Directory of Open Access Journals (Sweden)

    Antonia eGonzález-Garrido

    2015-12-01

    Full Text Available Acid-sensing ion channels (ASICs are activated by an increase in the extracellular proton concentration. There are four genes (ASIC1-4 that encode six subunits, and they are involved in diverse neuronal functions, such as mechanosensation, learning and memory, nociception, and modulation of retinal function. In this study, we characterize the ASIC currents of spiral ganglion neurons (SGNs. These ASIC currents are primarily carried by Na+, exhibit fast activation and desensitization, display a pH50 of 6.2 and are blocked by amiloride, indicating that these are ASIC currents. The ASIC currents were further characterized using several pharmacological tools. Gadolinium and acetylsalicylic acid reduced these currents, and FMRFamide, zinc (at high concentrations and N,N,N’,N’–tetrakis-(2-piridilmetil-etilendiamina (TPEN increased them, indicating that functional ASICs are composed of the subunits ASIC1, ASIC2 and ASIC3. Neomycin and streptomycin reduced the desensitization rate of the ASIC current in SGNs, indicating that ASICs may contribute to the ototoxic action of aminoglycosides. RT-PCR of the spiral ganglion revealed significant expression of all ASIC subunits. By immunohistochemistry the expression of the ASIC1a, ASIC2a, ASIC2b and ASIC3 subunits was detected in SGNs. Although only a few SGNs exhibited action potential firing in response to an acidic stimulus, protons in the extracellular solution modulated SGN activity during sinusoidal stimulation. Our results show that protons modulate the excitability of SGNs via ASICs.

  19. Acid-Sensing Ion Channels Expression, Identity and Role in the Excitability of the Cochlear Afferent Neurons

    Science.gov (United States)

    González-Garrido, Antonia; Vega, Rosario; Mercado, Francisco; López, Iván A.; Soto, Enrique

    2015-01-01

    Acid-sensing ion channels (ASICs) are activated by an increase in the extracellular proton concentration. There are four genes (ASIC1-4) that encode six subunits, and they are involved in diverse neuronal functions, such as mechanosensation, learning and memory, nociception, and modulation of retinal function. In this study, we characterize the ASIC currents of spiral ganglion neurons (SGNs). These ASIC currents are primarily carried by Na+, exhibit fast activation and desensitization, display a pH50 of 6.2 and are blocked by amiloride, indicating that these are ASIC currents. The ASIC currents were further characterized using several pharmacological tools. Gadolinium and acetylsalicylic acid reduced these currents, and FMRFamide, zinc (at high concentrations) and N,N,N’,N’–tetrakis-(2-piridilmetil)-ethylenediamine increased them, indicating that functional ASICs are composed of the subunits ASIC1, ASIC2, and ASIC3. Neomycin and streptomycin reduced the desensitization rate of the ASIC current in SGNs, indicating that ASICs may contribute to the ototoxic action of aminoglycosides. RT-PCR of the spiral ganglion revealed significant expression of all ASIC subunits. By immunohistochemistry the expression of the ASIC1a, ASIC2a, ASIC2b, and ASIC3 subunits was detected in SGNs. Although only a few SGNs exhibited action potential firing in response to an acidic stimulus, protons in the extracellular solution modulated SGN activity during sinusoidal stimulation. Our results show that protons modulate the excitability of SGNs via ASICs. PMID:26733809

  20. Valproic Acid

    Science.gov (United States)

    ... acid is in a class of medications called anticonvulsants. It works by increasing the amount of a ... older (about 1 in 500 people) who took anticonvulsants such as valproic acid to treat various conditions ...

  1. Ascorbic Acid

    Science.gov (United States)

    Ascorbic acid is used to prevent and treat scurvy, a disease caused by a lack of vitamin C ... Ascorbic acid comes in extended-release (long-acting) capsules and tablets, lozenges, syrup, chewable tablets, and liquid drops ...

  2. Amino acids

    Science.gov (United States)

    ... this page: //medlineplus.gov/ency/article/002222.htm Amino acids To use the sharing features on this page, please enable JavaScript. Amino acids are organic compounds that combine to form proteins . ...

  3. Fatty acids - trans fatty acids

    Science.gov (United States)

    The data supporting a negative effect of dietary trans fatty acids on cardiovascular disease risk is consistent. The primary dietary sources of trans fatty acids include partially hydrogenated fat and rudiment fat. The adverse effect of trans fatty acids on plasma lipoprotein profiles is consisten...

  4. Ibotenic acid and thioibotenic acid

    DEFF Research Database (Denmark)

    Hermit, Mette B; Greenwood, Jeremy R; Nielsen, Birgitte

    2004-01-01

    In this study, we have determined and compared the pharmacological profiles of ibotenic acid and its isothiazole analogue thioibotenic acid at native rat ionotropic glutamate (iGlu) receptors and at recombinant rat metabotropic glutamate (mGlu) receptors expressed in mammalian cell lines....... Thioibotenic acid has a distinct pharmacological profile at group III mGlu receptors compared with the closely structurally related ibotenic acid; the former is a potent (low microm) agonist, whereas the latter is inactive. By comparing the conformational energy profiles of ibotenic and thioibotenic acid...... with the conformations preferred by the ligands upon docking to mGlu1 and models of the other mGlu subtypes, we propose that unlike other subtypes, group III mGlu receptor binding sites require a ligand conformation at an energy level which is prohibitively expensive for ibotenic acid, but not for thioibotenic acid...

  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...... in acidic organelles, implying a different toxic mechanism of action. We propose that rapid induction of LBs, an indicator of phospholipidosis, should be included in the future toxicity profile of OA....

  6. Folic Acid

    Science.gov (United States)

    ... damage. 10 Do I need folic acid after menopause? Yes. Women who have gone through menopause still need 400 micrograms of folic acid every ... United States: 2003–2006 . American Journal of Clinical Nutrition; 91(1): 231–237. Hamner, H.C., Cogswell, ...

  7. Direct and indirect inactivation of tumor cell protective catalase by salicylic acid and anthocyanidins reactivates intercellular ROS signaling and allows for synergistic effects.

    Science.gov (United States)

    Scheit, Katrin; Bauer, Georg

    2015-03-01

    Salicylic acid and anthocyanidins are known as plant-derived antioxidants, but also can provoke paradoxically seeming prooxidant effects in vitro. These prooxidant effects are connected to the potential of salicylic acid and anthocyanidins to induce apoptosis selectively in tumor cells in vitro and to inhibit tumor growth in animal models. Several epidemiological studies have shown that salicylic acid and its prodrug acetylsalicylic acid are tumor-preventive for humans. The mechanism of salicylic acid- and anthocyanidin-dependent antitumor effects has remained enigmatic so far. Extracellular apoptosis-inducing reactive oxygen species signaling through the NO/peroxynitrite and the HOCl signaling pathway specifically induces apoptosis in transformed cells. Tumor cells have acquired resistance against intercellular reactive oxygen species signaling through expression of membrane-associated catalase. Here, we show that salicylic acid and anthocyanidins inactivate tumor cell protective catalase and thus reactive apoptosis-inducing intercellular reactive oxygen species signaling of tumor cells and the mitochondrial pathway of apoptosis Salicylic acid inhibits catalase directly through its potential to transform compound I of catalase into the inactive compound II. In contrast, anthocyanidins provoke a complex mechanism for catalase inactivation that is initiated by anthocyanidin-mediated inhibition of NO dioxygenase. This allows the formation of extracellular singlet oxygen through the reaction between H(2)O(2) and peroxynitrite, amplification through a caspase8-dependent step and subsequent singlet oxygen-mediated inactivation of catalase. The combination of salicylic acid and anthocyanidins allows for a remarkable synergistic effect in apoptosis induction. This effect may be potentially useful to elaborate novel therapeutic approaches and crucial for the interpretation of epidemiological results related to the antitumor effects of secondary plant compounds.

  8. Electrogenerated chemiluminescence quenching of Ru(bpy){sub 3} {sup 2+} (bpy=2,2 Prime -bipyridine) in the presence of acetaminophen, salicylic acid and their metabolites

    Energy Technology Data Exchange (ETDEWEB)

    Haslag, Catherine S. [Department of Chemistry, Missouri State University, Springfield, Missouri 65897 (United States); Richter, Mark M., E-mail: MarkRichter@missouristate.edu [Department of Chemistry, Missouri State University, Springfield, Missouri 65897 (United States)

    2012-03-15

    Quenching of Ru(bpy) {sub 3}{sup 2+} (bpy=2,2 Prime -bipyridine) coreactant electrogenerated chemiluminescence (ECL) has been observed in the presence of acetaminophen, salicylic acid and related complexes. However, no quenching is observed with the acetylsalicylic acid. In most instances, quenching is observed with 100-fold excess of quencher (compared to ECL luminophore) with complete quenching observed between 10,000 and 100,000 fold excess. Fluorescence and UV-vis experiments coupled with bulk electrolysis support the formation of benzoquinone products upon electrochemical oxidation. The mechanism of quenching may involve the interaction of the electrochemically generated benzoquinone species with (i) the {sup Low-Asterisk }Ru(bpy){sub 3}{sup 2+} excited state or (ii) highly energetic coreactant radicals. - Highlights: Black-Right-Pointing-Triangle Efficient quenching of the electrogenerated chemiluminescence is observed. Black-Right-Pointing-Triangle Acetaminophen, salicylic acid and related compounds can be detected. Black-Right-Pointing-Triangle The mechanism of quenching involves benzoquinones formed upon electrolysis.

  9. Solid-state 17O NMR of pharmaceutical compounds: salicylic acid and aspirin.

    Science.gov (United States)

    Kong, Xianqi; Shan, Melissa; Terskikh, Victor; Hung, Ivan; Gan, Zhehong; Wu, Gang

    2013-08-22

    We report solid-state NMR characterization of the (17)O quadrupole coupling (QC) and chemical shift (CS) tensors in five site-specifically (17)O-labeled samples of salicylic acid and o-acetylsalicylic acid (Aspirin). High-quality (17)O NMR spectra were obtained for these important pharmaceutical compounds under both static and magic angle spinning (MAS) conditions at two magnetic fields, 14.0 and 21.1 T. A total of 14 (17)O QC and CS tensors were experimentally determined for the seven oxygen sites in salicylic acid and Aspirin. Although both salicylic acid and Aspirin form hydrogen bonded cyclic dimers in the solid state, we found that the potential curves for the concerted double proton transfer in these two compounds are significantly different. In particular, while the double-well potential curve in Aspirin is nearly symmetrical, it is highly asymmetrical in salicylic acid. This difference results in quite different temperature dependencies in (17)O MAS spectra of the two compounds. A careful analysis of variable-temperature (17)O MAS NMR spectra of Aspirin allowed us to obtain the energy asymmetry (ΔE) of the double-well potential, ΔE = 3.0 ± 0.5 kJ/mol. We were also able to determine a lower limit of ΔE for salicylic acid, ΔE > 10 kJ/mol. These asymmetrical features in potential energy curves were confirmed by plane-wave DFT computations, which yielded ΔE = 3.7 and 17.8 kJ/mol for Aspirin and salicylic acid, respectively. To complement the solid-state (17)O NMR data, we also obtained solid-state (1)H and (13)C NMR spectra for salicylic acid and Aspirin. Using experimental NMR parameters obtained for all magnetic nuclei present in salicylic acid and Aspirin, we found that plane-wave DFT computations can produce highly accurate NMR parameters in well-defined crystalline organic compounds.

  10. Mefenamic Acid

    Science.gov (United States)

    ... any of the inactive ingredients in mefenamic acid capsules. Ask your pharmacist for a list of the inactive ingredients.tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking ...

  11. Acid Rain

    Science.gov (United States)

    Bricker, Owen P.; Rice, Karen C.; Dietrich, W.E.; Sposito, Garrison

    1997-01-01

    Acid deposition, or acid rain as it is more commonly referred to, has become a widely publicized environmental issue in the U.S. over the past decade. The term usually conjures up images of fish kills, dying forests, "dead" lakes, and damage to monuments and other historic artifacts. The primary cause of acid deposition is emission of S02 and NOx to the atmosphere during the combustion of fossil fuels. Oxidation of these compounds in the atmosphere forms strong acids - H2SO4 and HNO3 - which are returned to the Earth in rain, snow, fog, cloud water, and as dry deposition.Although acid deposition has only recently been recognized as an environmental problem in the U.S., it is not a new phenomenon (Cogbill & Likens 1974). As early as the middle of the 17th century in England, the deleterious effects of industrial emissions on plants, animals, and humans, and the atmospheric transport of pollutants between England and France had become issues of concern (Evelyn 1661, Graunt 1662). It is interesting that well over three hundred years ago in England, recommendations were made to move industry outside of towns and build higher chimneys to spread the pollution into "distant parts." Increasing the height of smokestacks has helped alleviate local problems, but has exacerbated others. In the U.S. the height of the tallest smokestack has more than doubled, and the average height of smokestacks has tripled since the 1950s (Patrick et al 1981). This trend occurred in most industrialized nations during the 20th century and has had the effect of transforming acid rain from a local urban problem into a problem of global scale.

  12. Screening procedure for detection of non-steroidal anti-inflammatory drugs and their metabolites in urine as part of a systematic toxicological analysis procedure for acidic drugs and poisons by gas chromatography-mass spectrometry after extractive methylation.

    Science.gov (United States)

    Maurer, H H; Tauvel, F X; Kraemer, T

    2001-01-01

    Non-steroidal anti-inflammatory drugs (NSAIDs) are widely used as analgesic and anti-rheumatic drugs, and they are often misused. A gas chromatographic-mass spectrometric (GC-MS) screening procedure was developed for their detection in urine as part of a systematic toxicological analysis procedure for acidic drugs and poisons after extractive methylation. The compounds were separated by capillary GC and identified by computerized MS in the full-scan mode. Using mass chromatography with the ions m/z 119, 135, 139, 152, 165, 229, 244, 266, 272, and 326, the possible presence of NSAIDs and their metabolites could be indicated. The identity of positive signals in such mass chromatograms was confirmed by comparison of the peaks underlying full mass spectra with the reference spectra recorded during this study. This method allowed the detection of therapeutic concentrations of acemetacin, acetaminophen (paracetamol), acetylsalicylic acid, diclofenac, diflunisal, etodolac, fenbufen, fenoprofen, flufenamic acid, flurbiprofen, ibuprofen, indometacin, kebuzone, ketoprofen, lonazolac, meclofenamic acid, mefenamic acid, mofebutazone, naproxen, niflumic acid, phenylbutazone, suxibuzone, tiaprofenic acid, tolfenamic acid, and tolmetin in urine samples. The overall recoveries of the different NSAIDs ranged between 50 and 80% with coefficients of variation of less than 15% (n = 5), and the limits of detection of the different NSAIDs were between 10 and 50 ng/mL (S/N = 3) in the full-scan mode. Extractive methylation has proved to be a versatile method for STA of various acidic drugs, poisons, and their metabolites in urine. It has also successfully been used for plasma analysis.

  13. High-Quality Metal–Organic Framework ZIF-8 Membrane Supported on Electrodeposited ZnO/2-methylimidazole Nanocomposite: Efficient Adsorbent for the Enrichment of Acidic Drugs

    Science.gov (United States)

    Wu, Mian; Ye, Huili; Zhao, Faqiong; Zeng, Baizhao

    2017-01-01

    Metal–organic framework (MOF) membranes have received increasing attention as adsorbents, yet the defects in most membrane structures greatly thwart their capacity performance. In this work, we fabricated a novel ZnO/2-methylimidazole nanocomposite with multiple morphology by electrochemical method. The nanocomposite provided sufficient and strong anchorages for the zeolitic imidazolate frameworks-8 (ZIF-8) membrane. Thus, a crack-free and uniform MOF membrane with high performance was successfully obtained. In this case, 2-methylimidazole was believed to react with ZnO to form uniform ZIF nuclei, which induced and guided the growth of ZIF-8 membrane. The as-prepared ZIF-8 membrane had large surface area and good thermal stability. As expected, it displayed high adsorption capacity for acidic drugs (e.g., ibuprofen, ketoprofen and acetylsalicylic acid) as they could interact through hydrophobic, hydrogen bonding and π-π stacking interaction. Accordingly, by coupling with gas chromatography the ZIF-8 membrane was successfully applied to the real-time dynamic monitoring of ibuprofen in patient’s urine.

  14. 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.

  15. Biochemical and pharmacological effects of dipyrone and its metabolites in model systems related to arachidonic acid cascade.

    Science.gov (United States)

    Weithmann, K U; Alpermann, H G

    1985-01-01

    The metabolites of dipyrone (metamizol, Novalgin) were compared with appropriate standard drugs for their influences on the pathways of the arachidonic acid metabolism. The drugs in this study had no significant effects on the lipoxygenase pathway in human neutrophils in vitro. The dipyrone metabolites 4-methylaminoantipyrine (MAAP) and 4-aminoantipyrine (AAP) inhibited prostaglandin synthesis in the 10(-3) to 10(-4) mol/l range thus being comparable to acetylsalicylic acid (ASA), whereas the two additional metabolites 4-acetylaminoantipyrine (AAAP) and 4-formylaminoantipyrine (FAAP) were practically inactive. This result is in accordance with the effects of the metabolites on the formation of oedema in the arthritis rat model, and supports published data showing that MAAP and AAP are the metabolites responsible for the clinical effects of dipyrone. Further systems in our study depending at least partially on the prostaglandin pathway were the release of antiaggregatory activity from rat aortae in vitro and the aggregation of human platelets induced by arachidonic acid in vitro. MAAP exhibits antiaggregatory activity (IC50 5 x 10(-6) mol/l), whereas the inhibitory effect on the vascular antiaggregatory release is much weaker. Compared to normals platelet aggregability ex vivo is enhanced in arthritic rats, but could significantly be lowered again by treatment of the rats with MAAP. A further system studied was the release of 6-keto-PGF1 alpha from rat mucosa in vitro and ex vivo. In vitro there is inhibition to be found with MAAP as well as with ASA. Ex vivo, however, dipyrone or MAAP slightly stimulates mucosal 6-keto-PGF1 alpha rather than inhibiting it, whereas ASA exerts inhibition, as expected.(ABSTRACT TRUNCATED AT 250 WORDS)

  16. Aspirin in pregnancy : clinical and biochemical studies

    NARCIS (Netherlands)

    H.A. Bremer (Henk)

    1994-01-01

    textabstractAspirin, acetylsalicylic acid, is the most frequently consumed drug in pregnancy,47 mostly taken without a prescription because of headache or a minor ailment. 226,277 Numerous preparations containing acetylsalicylic acid are freely available over the counter under a variety of proprieta

  17. Peptic ulcerations are related to systemic rather than local effects of low-dose aspirin.

    NARCIS (Netherlands)

    Oijen, M.G.H. van; Dieleman, J.P.; Laheij, R.J.F.; Sturkenboom, M.C.; Jansen, J.B.M.J.; Verheugt, F.W.A.

    2008-01-01

    BACKGROUND & AIMS: Effervescent calcium carbasalate is a calcium-salt of acetylsalicylic acid causing less local gastric damage than acetylsalicylic acid at high doses in healthy controls. The aim of the study was to investigate the incidence of peptic ulcers in a population-based cohort using bioeq

  18. Acetylsalicylzuur bij patienten met diabetes mellitus: niet voor primaire, wel voor secundaire preventie van hart-vaatziekten

    NARCIS (Netherlands)

    Klomp, C.M.; ten Cate, H.; Stehouwer, C.D.; Schaper, N.C.

    2009-01-01

    There is no consensus in international guidelines about the role of acetylsalicylic acid in primary prevention of cardiovascular events in patients with diabetes mellitus.Primary prevention trials suggest that in diabetic patients, acetylsalicylic acid has either no or less favourable effects in pre

  19. SYNTHESIS OF 1-(ACETYLSALICYLYL)-BENZOTRIAZOLE AND ITS REACTION WITH POLYVINYL ALCOHOL

    Institute of Scientific and Technical Information of China (English)

    GU Zhongwei; LI Fumian; FENG Xinde

    1983-01-01

    1-(Acetylsalicylyl)-benzotriazole, a new active amide of acetylsalicylic acid has been synthesized either from acetylsalicylic acid and benzotriazole using DCCI as condensation agent or via acetylsalicylyl chloride and benzotriazole in the presence of triethylamine. The obtained active amide reacted readily with the hydroxyl group of PVA to produce the acetylsalicylyl ester of PVA.

  20. Determination of Chlorogenic Acid and Acetylsalicylic Acid in Compound Cold Capsule by HPLC%高效液相色谱法测定复方感冒胶囊中绿原酸和乙酰水杨酸的含量

    Institute of Scientific and Technical Information of China (English)

    邢俊波; 曹红

    2005-01-01

    目的建立高效液相色谱法测定复方感冒胶囊中绿原酸和乙酰水杨酸的含量测定方法.方法采用SHIMADZU VP-ODS(250 mm × 4.6 mm,5μm)分析柱;流动相:乙腈-0.4%磷酸溶液(10:90)与乙腈-0.3%磷酸溶液(25:75);流速:1.0 mL/min;检测波长320 nm,进样10 μ L.结果绿原酸的线性范围为0.0524~0.2620μg,r2=1,平均回收率为1 03.87%,RSD=0.75%;乙酰水杨酸的线性范围为0.122~1.22 μ g,r2=0.9996,平均回收率为98.11%,RSD=3.33%(n=6).结论该法简便,结果可靠.

  1. Hydrofluoric acid poisoning

    Science.gov (United States)

    Fluorhydric acid ... stomach, or intestine have holes (perforations) from the acid. ... Hydrofluoric acid is especially dangerous. The most common accidents involving hydrofluoric acid cause severe burns on the skin ...

  2. Dehydroabietic acid

    Directory of Open Access Journals (Sweden)

    Xiao-Ping Rao

    2009-10-01

    Full Text Available The title compound [systematic name: (1R,4aS,10aR-7-isopropyl-1,4a-dimethyl-1,2,3,4,4a,9,10,10a-octahydrophenanthrene-1-carboxylic acid], C20H28O2, has been isolated from disproportionated rosin which is obtained by isomerizing gum rosin with a Pd-C catalyst.. Two crystallographically independent molecules exist in the asymmetric unit. In each molecule, there are three six-membered rings, which adopt planar, half-chair and chair conformations. The two cyclohexane rings form a trans ring junction with the two methyl groups in axial positions. The crystal structure is stabilized by intermolecular O—H...O hydrogen bonds.

  3. Aspirin’s Active Metabolite Salicylic Acid Targets High Mobility Group Box 1 to Modulate Inflammatory Responses

    Science.gov (United States)

    Choi, Hyong Woo; Tian, Miaoying; Song, Fei; Venereau, Emilie; Preti, Alessandro; Park, Sang-Wook; Hamilton, Keith; Swapna, G V T; Manohar, Murli; Moreau, Magali; Agresti, Alessandra; Gorzanelli, Andrea; De Marchis, Francesco; Wang, Huang; Antonyak, Marc; Micikas, Robert J; Gentile, Daniel R; Cerione, Richard A; Schroeder, Frank C; Montelione, Gaetano T; Bianchi, Marco E; Klessig, Daniel F

    2015-01-01

    Salicylic acid (SA) and its derivatives have been used for millennia to reduce pain, fever and inflammation. In addition, prophylactic use of acetylsalicylic acid, commonly known as aspirin, reduces the risk of heart attack, stroke and certain cancers. Because aspirin is rapidly de-acetylated by esterases in human plasma, much of aspirin’s bioactivity can be attributed to its primary metabolite, SA. Here we demonstrate that human high mobility group box 1 (HMGB1) is a novel SA-binding protein. SA-binding sites on HMGB1 were identified in the HMG-box domains by nuclear magnetic resonance (NMR) spectroscopic studies and confirmed by mutational analysis. Extracellular HMGB1 is a damage-associated molecular pattern molecule (DAMP), with multiple redox states. SA suppresses both the chemoattractant activity of fully reduced HMGB1 and the increased expression of proinflammatory cytokine genes and cyclooxygenase 2 (COX-2) induced by disulfide HMGB1. Natural and synthetic SA derivatives with greater potency for inhibition of HMGB1 were identified, providing proof-of-concept that new molecules with high efficacy against sterile inflammation are attainable. An HMGB1 protein mutated in one of the SA-binding sites identified by NMR chemical shift perturbation studies retained chemoattractant activity, but lost binding of and inhibition by SA and its derivatives, thereby firmly establishing that SA binding to HMGB1 directly suppresses its proinflammatory activities. Identification of HMGB1 as a pharmacological target of SA/aspirin provides new insights into the mechanisms of action of one of the world’s longest and most used natural and synthetic drugs. It may also provide an explanation for the protective effects of low-dose aspirin usage. PMID:26101955

  4. CLINICAL EXPERIENCE OF CANCER IMMUNOTHERAPY INTEGRATED WITH OLEIC ACID COMPLEXED WITH DE-GLYCOSYLATED VITAMIN D BINDING PROTEIN

    Directory of Open Access Journals (Sweden)

    Emma Ward

    2014-01-01

    Full Text Available Proteins highly represented in milk such as α-lactalbumin and lactoferrin bind Oleic Acid (OA to form complexes with selective anti-tumor activity. A protein present in milk, colostrum and blood, vitamin D binding protein is the precursor of a potent Macrophage Activating Factor (GcMAF and in analogy with other OA-protein complexes, we proposed that OA-GcMAF could demonstrate a greater immunotherapeutic activity than that of GcMAF alone. We describe a preliminary experience treating patients with advanced cancers, often labelled as “incurable” with an integrative immunotherapy centred on OA-GcMAF. Patients with advanced cancer were treated at the Immuno Biotech Treatment Centre with OA-GcMAF-based integrative immunotherapy in combination with a very low carbohydrate, high protein diet, fermented milk products containing naturally produced GcMAF, vitamin D3 and low-dose acetylsalicylic acid. When the primary tumor or a metastasis could be measured by ultrasonographic techniques, we observed, on average, a decrease of tumor volume of approximately 25% in a week. We also observed a consistent increase in splenic blood flow that was interpreted in the context of generalised immune system activation and allowed to assess the degree of responsiveness of the individual patient. The results reported here are consistent with the results previously described in the experimental animal harbouring a human hepatocellular carcinoma as well as with the results reported for neoadjuvant chemotherapy. OA-protein complexes are bound to play a leading role in cancer therapy thanks to selectivity of antitumoral effects, absence of any side effects, safety and oral availability. We hypothesise that OA-GcMAF, combines the known anticancer effects OA-protein complexes with the well established immune stimulating effects of GcMAF.

  5. Method development and validation for optimised separation of salicylic, acetyl salicylic and ascorbic acid in pharmaceutical formulations by hydrophilic interaction chromatography and response surface methodology.

    Science.gov (United States)

    Hatambeygi, Nader; Abedi, Ghazaleh; Talebi, Mohammad

    2011-09-02

    This paper introduces a design of experiments (DOE) approach for method optimisation in hydrophilic interaction chromatography (HILIC). An optimisation strategy for the separation of acetylsalicylic acid, its major impurity salicylic acid and ascorbic acid in pharmaceutical formulations by HILIC is presented, with the aid of response surface methodology (RSM) and Derringer's desirability function. A Box-Behnken experimental design was used to build the mathematical models and then to choose the significant parameters for the optimisation by simultaneously taking both resolution and retention time as the responses. The refined model had a satisfactory coefficient (R²>0.92, n=27). The four independent variables studied simultaneously were: acetonitrile content of the mobile phase, pH and concentration of buffer and column temperature each at three levels. Of these, the concentration of buffer and its cross-product with pH had a significant, positive influence on all studied responses. For the test compounds, the best separation conditions were: acetonitrile/22 mM ammonium acetate, pH 4.4 (82:18, v/v) as the mobile phase and column temperature of 28°C. The methodology also captured the interaction between variables which enabled exploration of the retention mechanism involved. It would be inferred that the retention is governed by a compromise between hydrophilic partitioning and ionic interaction. The optimised method was further validated according to the ICH guidelines with respect to linearity and range, precision, accuracy, specificity and sensitivity. The robustness of the method was also determined and confirmed by overlying counter plots of responses which were derived from the experimental design utilised for method optimisation.

  6. [Teichoic acids from lactic acid bacteria].

    Science.gov (United States)

    Livins'ka, O P; Harmasheva, I L; Kovalenko, N K

    2012-01-01

    The current view of the structural diversity of teichoic acids and their involvement in the biological activity of lactobacilli has been reviewed. The mechanisms of effects of probiotic lactic acid bacteria, in particular adhesive and immunostimulating functions have been described. The prospects of the use of structure data of teichoic acid in the assessment of intraspecific diversity of lactic acid bacteria have been also reflected.

  7. Dietary non-nutrients and haemostasis in humans: effects of salicylates, flavonoids and ginger.

    NARCIS (Netherlands)

    Janssen, P.L.T.M.K.

    1997-01-01

    In this thesis we studied the content of acetylsalicylate and total salicylates in foods, and we studied the effects of the dietary non-nutrients salicylates and flavonoids and of certain foods on haemostatic parameters in humans.Acetylsalicylic acid -aspirin- irreversibly inhibits platelet cyclo-ox

  8. Plasma amino acids

    Science.gov (United States)

    Amino acids blood test ... types of methods used to determine the individual amino acid levels in the blood. ... test is done to measure the level of amino acids in the blood. An increased level of a ...

  9. POLYELEOSTEARIC ACID VESICLES

    Institute of Scientific and Technical Information of China (English)

    LI Zichen; XIE Ximng; FAN Qinghua; FANG Yifei

    1992-01-01

    α-Eleostearic acid and β-eleostearic acid formed vesicles in aqueous medium when an ethanol solutionofeleostearic acid was injected rapidly into a vigorously vortexed aqueous phase. Formation of the vesicles was demonstrated by electron microscopic observation and bromothymol blue encapsulation experiments. Polymerizations of the eleostearic acids in the formed vesicles carried out by UV irradiation produced poly-α-eleostearic acid and poly-β-eleostearic acid vesicles.

  10. Acid distribution in phosphoric acid fuel cells

    Energy Technology Data Exchange (ETDEWEB)

    Okae, I.; Seya, A.; Umemoto, M. [Fuji Electric Co., Ltd., Chiba (Japan)

    1996-12-31

    Electrolyte acid distribution among each component of a cell is determined by capillary force when the cell is not in operation, but the distribution under the current load conditions had not been clear so far. Since the loss of electrolyte acid during operation is inevitable, it is necessary to store enough amount of acid in every cell. But it must be under the level of which the acid disturbs the diffusion of reactive gases. Accordingly to know the actual acid distribution during operation in a cell is very important. In this report, we carried out experiments to clarify the distribution using small single cells.

  11. Gas-phase Acidities of Aspartic Acid, Glutamic Acid, and their Amino Acid Amides.

    Energy Technology Data Exchange (ETDEWEB)

    Li, Zhong; Matus, Myrna H; Velazquez, Hector A; Dixon, David A; Cassady, Carolyn J

    2007-02-14

    Gas-phase acidities (GA or ΔGacid) for the two most acidic common amino acids, aspartic acid and glutamic acid, have been determined for the first time. Because of the amide linkage’s importance in peptides and as an aid in studying side chain versus main chain deprotonation, aspartic acid amide and glutamic acid amide were also studied. Experimental GA values were measured by proton transfer reactions in an electrospray ionization/Fourier transform ion cyclotron resonance mass spectrometer. Calculated GAs were obtained by density functional and molecular orbital theory approaches. The best agreement with experiment was found at the G3MP2 level; the MP2/CBS and B3LYP/aug-cc-pVDZ results are 3–4 kcal/mol more acidic than the G3MP2 results. Experiment shows that aspartic acid is more acidic than glutamic acid by ca. 3 kcal/mol whereas the G3MP2 results show a smaller acidity difference of 0.2 kcal/mol. Similarly, aspartic acid amide is experimentally observed to be ca. 2 kcal/mol more acidic than glutamic acid amide whereas the G3MP2 results show a correspondingly smaller energy difference of 0.7 kcal/mol. The computational results clearly show that the anions are all ring-like structures with strong hydrogen bonds between the OH or NH2 groups and the CO2- group from which the proton is removed. The two amino acids are main-chain deprotonated. In addition, use of the COSMO model for the prediction of the free energy differences in aqueous solution gave values in excellent agreement with the most recent experimental values for pKa. Glutamic acid is predicted to be more acidic than aspartic acid in aqueous solution due to differential solvation effects.

  12. Novel mixed metal Ag(I)-Sb(III)-metallotherapeutics of the NSAIDs, aspirin and salicylic acid: Enhancement of their solubility and bioactivity by using the surfactant CTAB.

    Science.gov (United States)

    Gkaniatsou, E I; Banti, C N; Kourkoumelis, N; Skoulika, S; Manoli, M; Tasiopoulos, A J; Hadjikakou, S K

    2015-09-01

    The already known Ag(I)-Sb(III) compound of the formula {Ag(Ph3Sb)3(NO3)} (1) and two novel mixed metal Ag(I)-Sb(III) metallotherapeutics of the formulae {Ag(Ph3Sb)3(SalH)}(2) and {Ag(Ph3Sb)3(Asp)}(3) (SalH2=salicylic acid, AspH=aspirin or 2-acetylsalicylic acid and Ph3Sb=triphenyl antimony(III)) have been synthesised and characterised by m.p., vibrational spectroscopy (mid-FT-IR), (13)C-,(1)H-NMR, UV-visible (UV-vis) spectroscopic techniques, high resolution mass spectroscopy (HRMS) and X-ray crystallography. Compounds 1,-3 were treated with the surfactant cetyltrimethylammonium bromide (CTAB) in order to enhance their solubility and as a consequence their bioactivity. The resulting micelles a-c were characterised with X-ray powder diffraction (XRPD) analysis, X-ray fluorescence (XRF) spectroscopy, Energy-dispersive X-ray spectroscopy (EDX), conductivity, Thermal gravimetry-differential thermal analysis (TG-DTA), and atomic absorption. Compounds 1-3 and the relevant micelles a-c were evaluated for their in vitro cytotoxic activity against human cancer cell lines: MCF-7 (breast, estrogen receptor (ER) positive), MDA-MB-231 (breast, ER negative) and MRC-5 (normal human fetal lung fibroblast cells) with sulforhodamine B (SRB) colorimetric assay. The results show significant increase in the activity of micelles compared to that of the initial compounds. Moreover, micelles exhibited lower activity against normal cells than tumor cells. The binding affinity of a-c towards the calf thymus (CT)-DNA, lipoxygenase (LOX) and glutathione (GSH) was studied by the fluorescent emission light and UV-vis spectroscopy.

  13. Gas-phase acidities of aspartic acid, glutamic acid, and their amino acid amides

    Science.gov (United States)

    Li, Zhong; Matus, Myrna H.; Velazquez, Hector Adam; Dixon, David A.; Cassady, Carolyn J.

    2007-09-01

    Gas-phase acidities (GA or [Delta]Gacid) for the two most acidic common amino acids, aspartic acid and glutamic acid, have been determined for the first time. Because of the amide linkage's importance in peptides and as an aid in studying side chain versus main chain deprotonation, aspartic acid amide and glutamic acid amide were also studied. Experimental GA values were measured by proton transfer reactions in an electrospray ionization/Fourier transform ion cyclotron resonance mass spectrometer. Calculated GAs were obtained by density functional and molecular orbital theory approaches. The best agreement with experiment was found at the G3MP2 level; the MP2/CBS and B3LYP/aug-cc-pVDZ results are 3-4 kcal/mol more acidic than the G3MP2 results. Experiment shows that aspartic acid is more acidic than glutamic acid by ca. 3 kcal/mol whereas the G3MP2 results show a smaller acidity difference of 0.2 kcal/mol. Similarly, aspartic acid amide is experimentally observed to be ca. 2 kcal/mol more acidic than glutamic acid amide whereas the G3MP2 results show a correspondingly smaller energy difference of 0.7 kcal/mol. The computational results clearly show that the anions are all ring-like structures with strong hydrogen bonds between the OH or NH2 groups and the CO2- group from which the proton is removed. The two amino acids are main-chain deprotonated. In addition, use of the COSMO model for the prediction of the free energy differences in aqueous solution gave values in excellent agreement with the most recent experimental values for pKa. Glutamic acid is predicted to be more acidic than aspartic acid in aqueous solution due to differential solvation effects.

  14. Acid Thunder: Acid Rain and Ancient Mesoamerica

    Science.gov (United States)

    Kahl, Jonathan D. W.; Berg, Craig A.

    2006-01-01

    Much of Mesoamerica's rich cultural heritage is slowly eroding because of acid rain. Just as water dissolves an Alka-Seltzer tablet, acid rain erodes the limestone surfaces of Mexican archaeological sites at a rate of about one-half millimeter per century (Bravo et al. 2003). A half-millimeter may not seem like much, but at this pace, a few…

  15. Drug: D07582 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available etic ATC code: A01AD05 B01AC06 N02BA01 cyclooxygenase-1 (COX-1) inhibitor [HSA:5742] [KO:K00509]; cyclooxygenase...N02BA01] D07582 Aspirin sodium cyclooxygenase-2 (COX-2) [HSA:5743] [KO:K11987] Acetylsalicylic acid [ATC:A01... N02BA01 Acetylsalicylic acid D07582 Aspirin sodium Target-based classification of drugs [BR:br08310] Enzymes Oxidoreductases cycloox...ygenase-1 (COX-1) [HSA:5742] [KO:K00509] Acetylsalicylic acid [ATC:A01AD05 B01AC06

  16. Amino Acid Metabolism Disorders

    Science.gov (United States)

    ... this process. One group of these disorders is amino acid metabolism disorders. They include phenylketonuria (PKU) and maple syrup urine disease. Amino acids are "building blocks" that join together to form ...

  17. Catalytic Synthesis Lactobionic Acid

    Directory of Open Access Journals (Sweden)

    V.G. Borodina

    2014-07-01

    Full Text Available Gold nanoparticles are obtained, characterized and deposited on the carrier. Conducted catalytic synthesis of lactobionic acid from lactose. Received lactobionic acid identify on the IR spectrum.

  18. Omega-3 Fatty Acids

    Science.gov (United States)

    Omega-3 fatty acids are used together with lifestyle changes (diet, weight-loss, exercise) to reduce the ... the blood in people with very high triglycerides. Omega-3 fatty acids are in a class of ...

  19. Omega-6 Fatty Acids

    Science.gov (United States)

    Omega-6 fatty acids are types of fats. Some types are found in vegetable oils, including corn, evening primrose seed, safflower, and soybean oils. Other types of omega-6 fatty acids are found in black currant ...

  20. Lactic acid test

    Science.gov (United States)

    ... this page: //medlineplus.gov/ency/article/003507.htm Lactic acid test To use the sharing features on this page, please enable JavaScript. Lactic acid is mainly produced in muscle cells and red ...

  1. Análise dos traçados de ondas da agregação plaquetária em pacientes com doenças cardiovasculares em uso do ácido acetil salicílico comparados a doadores de sangue Analysis of the waves and aggregation patterns in patients with cardiovascular diseases in using acetylsalicylic acid compared blood donors

    Directory of Open Access Journals (Sweden)

    Patrícia S. M. Bernardi

    2004-12-01

    Full Text Available A agregação plaquetária avalia a função das plaquetas através de diferentes vias de ativação plaquetária in vitro, fornecendo traçados de ondas equivalentes à propriedade física dessa agregação. Sabendo-se que a aspirina acetila irrever­sivelmente a enzima cicloxigenase prevenindo a geração de tromboxana A2, potente ativador da agregação plaquetária, esta droga tem sido analisada há mais de trinta anos na clínica médica em pacientes com doenças cardiovasculares como uma potente droga antitrombótica. Foram nossos objetivos obter traçados de ondas correspondentes às fases da agregação plaquetária para nossa padronização utilizando nosso grupo controle de doadores de sangue e compará-las com nosso grupo estudo, frente a diferentes agentes agonistas em diferentes concentrações: ADP 1µM e 3µM; AA, 0,5mM; ADR, 0,05 mg/mL, 0,025 mg/mL e 0,010 mg/mL. Os grupos analisados foram constituídos por 41 cardíacos e 40 doadores de sangue considerados controle. Dos cardíacos, 33 faziam uso regular do AAS na concentração de 200 mg/dia e oito na concentração de 100 mg/dia, sendo todos considerados hipertensos. A padronização da agregometria estava na dependência do encontro de traçados correspondentes a ondas de agregação, sendo esses obtidos em porcentagem no tempo de cinco minutos estandartizados pelo aparelho utilizado. Comparando os resultados entre os pacientes e o grupo controle, foi possível observar que, na presença dos agentes agregantes ADP 1µM e ADP 3 µM, ADR 0,05 mg/mL, 0,025mg/mL e 0,010 mg/mL, os pacientes apresentaram 1ª onda, mas não 2ª onda. Por sua vez, no caso do AA 0,5 mM não houve o encontro de traçados de ondas.Platelet aggregation illustrates the function of the platelets by different ways of in vitro platelet activation providing wave traces equivalent to the physical proprieties of this aggregation. It is well known that aspirin irreversibly blocks the cyclooxygenase enzyme preventing the release of thromboxane A2, a potent activator of platelet aggregation. This drug has been evaluated for more than thirty years as a potent antithrombotic drug in patients with cardiovascular diseases. Our objective was to obtain wave traces corresponding to platelet aggregation phases for standardization purposes using blood donors as a control group and comparing the results with a study group using different agonistic agents at different concentrations: ADP 1 µM and 3 µM; AA 0.5 mM and ADR at 0.05 mg/mL, 0.025 mg/mL and 0.010 mg/mL. The analyzed groups were composed of 41 cardiac patients and 40 blood donors. Among the cardiac patients, 33 regularly used 200 mg of ASA per day and 8 patients normally used 100 mg of ASA per day, all of whom were considered hypertensive. The pattern of aggregation was dependent on conjunction traces corresponding to aggregation waves. A percentage at 5 minutes was obtained with these traces established by the equipment used. In our work, comparing the results among analysed patients and the control group, it was possible to observe that in the presence of the aggregating agents ADP 1µM and ADP 3µM; ADR 0.05 mg/mL, 0.025 mg/mL and 0.010 mg/mL the patients showed the first wave but no second wave aggregation. However, in respect to AA 0.5 mM the conjunction of the trace waves was not seen.

  2. Solid Acid Catalyst Loaded on Bentonite and Its Catalysis of the Synthesis of Acetylsalicylate%膨润土负载型固体酸的制备、表征及催化乙酰水杨酸合成反应

    Institute of Scientific and Technical Information of China (English)

    王红斌; 施金榆; 宁平; 杨敏; 冯桂权

    2009-01-01

    用无水浸渍法制备了膨润土负载型固体酸催化剂,以乙酰水杨酸合成反应为探针考察了制备及反应条件对催化性能的影响,通过XRD、DTA及离子酸度等分析测试技术对催化剂进行表征分析. 结果表明,当用体积分数10%HCl浸泡12 h以上,负载5.0 mmol/g ZnCl2或4.0 mmol/g CuCl2,550 ℃下焙烧活化3 h,制备固体酸及固体酸用量为水杨酸的5%,水杨酸和乙酸酐投料摩尔比为1∶ 2,反应温度为80~90 ℃,反应时间为1 h,产率可达96.6%. 制备的固体酸催化剂可替代浓硫酸并能重复使用.

  3. Preparation of Y2P2W18O62·nH2O/4A Zeolite and Its Application for Catalytic Synthesis of Acetylsalicylic Acid%Y2P2W18O62·nH2O/4A-分子筛的制备及催化合成乙酰水杨酸

    Institute of Scientific and Technical Information of China (English)

    曹小华

    2016-01-01

    以4A-分子筛为载体,Dawson结构磷钨酸钇(Y2P2W18O62·nH2O)为活性组分,采用浸渍法制备出负载型40%Y2P2W18 O62· nH2O/4A-分子筛,并通过FT IR、EDS、SEM、NH3-TPD及N2吸附-脱附等方法对催化剂进行表征.将其用于催化水杨酸和乙酸酐反应制备乙酰水杨酸,考察了各因素对反应的影响.结果表明,负载前后磷钨酸钇均保持Dawson结构,Y2P2W18O62·nH2O和40%Y2P2W18O62·nH2O/4A-分子筛均呈球形,负载后催化剂的比表面积增大,酸强度和酸量均明显提高.在优化反应条件(水杨酸与乙酸酐摩尔比为1∶3,反应时间为30min,催化剂用量为反应物质量分数的2.3%)下,乙酰水杨酸收率为95.2%.催化剂重复使用6次,乙酰水杨酸收率仍保持为77.9%.

  4. Synthesis and antithrombotic activity of acetylsalicyl ferulic acid-coupling furoxans and nitrates%乙酰水杨酰阿魏酸与呋咱氮氧化物和硝酸酯偶联物的合成及其抗血栓作用

    Institute of Scientific and Technical Information of China (English)

    周洲; 蒋丽媛; 张奕华; 季晖; 孙易; 彭司勋

    2006-01-01

    目的 研究NO供体型阿司匹林衍生物的合成和抗血栓活性,寻找新型抗血栓药物.方法 阿司匹林经阿魏酸分别与呋咱氮氧化物和硝酸酯连接得到目标化合物;通过体外、体内血小板聚集试验和大鼠动静脉旁路血栓试验对新化合物进行抗血栓作用初筛.结果 合成了14个新化合物I1-14,其结构经MS,IR,1H NMR和元素分析确证;药理初筛结果表明,部分化合物在体内、体外均显示出较好的抗血栓活性.结论 乙酰水杨酰阿魏酸与呋咱氮氧化物和硝酸酯偶联物可作为抗血栓先导物,值得深入研究.

  5. Synthesis and Antithrombotic Activity of Acetylsalicyl p-Coumaric Acid Coupled with Furoxans and Nitrates%乙酰水杨酰对羟基桂皮酸与呋咱氮氧化物和硝酸酯偶联物的合成及其抗血栓作用

    Institute of Scientific and Technical Information of China (English)

    周洲; 蒋丽媛; 张奕华; 季晖; 孙易; 彭司勋

    2006-01-01

    对羟基桂皮酸酚羟基经保护后与相应的羟基呋咱氮氧化物酯化,酯化物脱保护,再与阿司匹林缩合得Ⅱ1~Ⅱ3;对羟基桂皮酸与相应二溴烷烃作用,再经阿司匹林酯化,得到的溴代烷基酯与硝酸银反应得Ⅱ4~Ⅱ4;酚羟基保护的对羟基桂皮酸与异山梨醇单硝酸酯酯化,脱保护后与阿司匹林缩合得Ⅱ8.目标物Ⅱ1~Ⅱ8均经MS,IR,1HNMR和元素分析确证,并通过大小鼠体内外抗血栓活性初筛,结果表明,多数目标物显示与阿司匹林相当的抗血栓活性,Ⅱ6活性优于阿司匹林.

  6. H6P2W18O62/MCM-41催化剂的制备、表征及其催化合成乙酰水杨酸%Preparation and Characterization of H6P2W18O62/MCM-41 Catalyst for Acetylsalicylic Acid Synthesis

    Institute of Scientific and Technical Information of China (English)

    曹小华; 王原平; 雷艳虹; 徐常龙; 占昌朝

    2014-01-01

    采用浸渍法将Dawson结构的磷钨酸H6P2W 18O62(简写为P2W18)负载在MCM-41分子筛上,制备出新型P2W18/MCM-41催化剂;采用FTIR,XRD,SEM,EDS等方法对催化剂进行了表征.表征结果显示,P2W18/MCM-41催化剂既保持了MCM-41分子筛的孔道结构,又保持了P2W18的Dawson结构.同时研究了P2W18/MCM-41催化剂对乙酰水杨酸合成反应的活性,通过正交实验确定了优化工艺条件:n(水杨酸)∶n(乙酸酐)=1.0∶1.5、P2W18/MCM-41催化剂用量2.7%(基于反应物的质量)、反应温度80℃、反应时间10 min.在此优化条件下,乙酰水杨酸收率为88.1%.P2W18/MCM-41催化剂重复使用5次,乙酰水杨酸收率仍可达76.7%.

  7. Injuria pulmonar aguda en la intoxicación por ácido acetilsalicílico: Caso clínico y revisión bibliográfica Acute lung injury due to acetylsalicylic acid poisoning: Case report and review

    Directory of Open Access Journals (Sweden)

    Victoria A Di Nardo

    2012-07-01

    Full Text Available La intoxicación por salicilatos frecuentemente no es tenida en cuenta como causa de edema pulmonar no cardiogénico y de alteración del sensorio en pacientes adultos. Se describe el caso de una mujer de 52 años de edad, la cual presentó dos episodios de edema pulmonar no cardiogénico habiendo requerido para su manejo, asistencia ventilatoria mecánica. La presentación clínica de la intoxicación fue reconocida al ingreso al servicio de urgencias y llevó al diagnóstico correcto. Se le realizó hemodiálisis y alcalinización urinaria llevando a una rápida resolución del edema pulmonar. Varios aspectos de la presentación clínica sugirieron que la paciente tenía una intoxicación crónica, una condición que a menudo no es diagnosticada oportunamente, lo que contribuye al aumento de la morbi-mortalidad en estos pacientes. Frente a un caso de edema pulmonar agudo no cardiogénico debe considerarse la posibilidad de intoxicación con salicilatos, porque la institución rápida de una terapia apropiada, incluyendo la hemodiálisis, una vez establecido el diagnóstico, es un factor determinante de los resultados en esta grave intoxicación.Salicylate intoxication is frequently overlooked as a cause of noncardiogenic pulmonary edema and altered mental status in adult patients. We described the case of a 52 years-old woman who presented two episodes of recurrent non-cardiogenic pulmonary edema requiring intubation. On admission, recognition of the clinical syndrome in the emergency department led to the correct diagnosis of salicylate intoxication. The patient was successfully treated with hemodialysis and urinary alkalinization, leading to rapid resolution of pulmonary edema and extubation. Several aspects of the clinical presentation suggest that the patient suffered from chronic salicylism, a condition often misdiagnosed or diagnosed late in the course of disease, contributing to substantial morbidity and mortality in these patients. This poisoning should be considered in the differential diagnosis of acute pulmonary edema not cardiogenic and altered sensorium because rapid institution of appropriate therapy, including hemodialysis, once the diagnosis is established is an important determinant of outcome in this serious disorder.

  8. BAP, 2,4-D e ácido acetilsalicílico na indução e diferenciação de calos em anteras de Coffea arabica L BAP, 2,4-D and acetyl-salicylic acid on the callus induction and differentiation in Coffea arabica L. anthers

    Directory of Open Access Journals (Sweden)

    Adelaide Siqueira Silva

    2009-10-01

    Full Text Available O melhoramento genético do cafeeiro por meio de métodos convencionais é um processo demorado para se obter uma nova cultivar. A redução desse tempo é possível através da produção de linhagens homozigóticas, oriundas de dihaplóides obtidas através da cultura de anteras. Objetivou-se aplicar a técnica da cultura de anteras em diferentes cvs. de Coffea arabica L. para induzir a formação de calos e regenerar plântulas di-haplóides, com uso de reguladores vegetais. Os experimentos foram conduzidos no laboratório de Biotecnologia Vegetal da Universidade Federal de Uberlândia (UFU. Anteras das cultivares Mundo Novo LCP-379-19 e Catuaí Vermelho H2077-2-5-44 foram inoculadas em meio MS suplementado com 2,0 mg L-1 de 2,4-D e AAS, nas concentrações de 0; 8; 16; 32 e 64 mg L-1. Calos de 'Catuaí Vermelho 44' foram subcultivados em meio MS acrescido de diferentes concentrações de BAP (0; 2; 4 e 8 mg L-1 e 2,4-D (0; 1; 2 e 4 mg L-1. Tanto para as cvs. Mundo Novo quanto para Catuaí Vermelho 44 o aumento das concentrações de AAS diminuiu a formação de próembrióides nos calos e somente o 2,4-D foi capaz de promover a formação de calos friáveis, porém o equilíbrio da auxina e da citocinina utilizadas no trabalho, favoreceram a produção de calos friáveis.Coffee plant breeding through conventional methods demands a long time to obtain new cultivars. The reduction of this period is possible through the production of homozygous lines, from dihaploids obtained via anther culture. The aim of this study was to apply the anther culture technique on different C. arabica L. cultivars to induce calli formation and to regenerate dihaploid seedlings with the use of plant growth regulators. The experiments were accomplished in the Plant Biotechnology laboratory at Uberlândia Federal University (UFU. Anthers of the cultivars Mundo Novo LCP-379-19 and Catuaí Vermelho H2077-2-5-44 were inoculated on MS medium supplemented with 2.0 mg L-1 2,4-D and ASA at 0, 8, 16, 32 or 64 mg L-1. 'Catuaí Vermelho 44' calli were subcultured on MS supplemented with different concentrations of BAP (0, 2, 4 or 8 mg L-1 and 2,4-D (0, 1, 2 or 4 mg L-1. The increase in ASA concentrations decreased the pro-embryoid formation on calli of both cultivars and only 2,4-D promoted the formation of friable calli. However, the balance of auxin and cytokinin used in this study favored the production of friable calli.

  9. 急性冠脉综合征采用氯吡格雷和阿司匹林治疗后引起的出血并发症%Bleeding Complications after Treatment with Clopidogrel and Acetylsalicylic Acid after Acute Coronary Syndrome

    Institute of Scientific and Technical Information of China (English)

    Kjaer; J; Larsen; CH; Poulsen; TS

    2006-01-01

    介绍:CURE(the Clopidogrel in Unstable Angina to Prevent Recurrent Events,氯吡格雷预防不稳定型心绞痛复发事件)研究显示不稳定型心绞痛(UAP)和非ST段抬高的心肌梗死(NSTEMI)患者联合使用阿司匹林(ASA)和氯吡格雷的益处。我们试图评价在一些未选择的丹麦患者中引入CURE标准是否增加出血的危险。

  10. Determination of lysine acetylsalicylate granules and its related substance salicylic acid by HPLC%高效液相色谱法测定赖氨匹林颗粒剂含量及其降解产物水杨酸的控制

    Institute of Scientific and Technical Information of China (English)

    郑国钢; 方滢芝

    2000-01-01

    目的:采用高效液相色谱法测定赖氨匹林颗粒剂含量并对其降解产物水杨酸进行控制.方法:以AlltimaC18柱为分析柱,甲醇-0.1%三乙胺溶液(1:1,冰醋酸调pH至3.5)为流动相,检测波长为280nm,以峰面积外标法计算.结果:赖氨匹林平均回收率为100.0%,RSD=0.47%(n=11);水杨酸平均回收率为100.3%,RSD=1.15%(n=6).结论:本法简便、快速、结果准确、可靠.

  11. 微波辐射Dawson结构多金属氧酸盐催化合成乙酰水杨酸的研究%Synthesis of Acetylsalicylic Acid Catalyzed by Substituted Dawson-Type Polyoxometa-lates under Microwave Irradiation

    Institute of Scientific and Technical Information of China (English)

    孙德武; 林险峰

    2009-01-01

    以Dawson结构多金属氧酸盐为催化剂,采用微波技术,用水杨酸和乙酸酐为原料直接合成乙酰水杨酸.考虑了不同Dawson结构多金属氧酸盐催化剂及最佳催化剂用量、水杨酸和乙酸酐物料配比、微波辐射功率以及辐射时间等对反应转化率的影响,为选择最佳合成条件提供了理论基础.

  12. Folic Acid Quiz

    Science.gov (United States)

    ... folic acid 9. A woman should be taking folic acid if she: A is planning a pregnancy B is capable of becoming pregnant, even if ... Answer: D CORRECT: A woman should be taking folic acid if she is planning a pregnancy, is capable of becoming pregnant (even if she ...

  13. Immunoglobulin and fatty acids

    DEFF Research Database (Denmark)

    2009-01-01

    The present invention relates to a composition comprising 0.1-10 w/w % immunoglobulin (Ig), 4-14 w/w % saturated fatty acids, 4-14 w/w % mono-unsaturated fatty acids and 0-5 w/w % poly-unsaturated fatty acids, wherein the weight percentages are based on the content of dry matter in the composition...

  14. Acid Rain Study Guide.

    Science.gov (United States)

    Hunger, Carolyn; And Others

    Acid rain is a complex, worldwide environmental problem. This study guide is intended to aid teachers of grades 4-12 to help their students understand what acid rain is, why it is a problem, and what possible solutions exist. The document contains specific sections on: (1) the various terms used in conjunction with acid rain (such as acid…

  15. The Acid Rain Reader.

    Science.gov (United States)

    Stubbs, Harriett S.; And Others

    A topic which is often not sufficiently dealt with in elementary school textbooks is acid rain. This student text is designed to supplement classroom materials on the topic. Discussed are: (1) "Rain"; (2) "Water Cycle"; (3) "Fossil Fuels"; (4) "Air Pollution"; (5) "Superstacks"; (6) "Acid/Neutral/Bases"; (7) "pH Scale"; (8) "Acid Rain"; (9)…

  16. Acidic Ionic Liquids.

    Science.gov (United States)

    Amarasekara, Ananda S

    2016-05-25

    Ionic liquid with acidic properties is an important branch in the wide ionic liquid field and the aim of this article is to cover all aspects of these acidic ionic liquids, especially focusing on the developments in the last four years. The structural diversity and synthesis of acidic ionic liquids are discussed in the introduction sections of this review. In addition, an unambiguous classification system for various types of acidic ionic liquids is presented in the introduction. The physical properties including acidity, thermo-physical properties, ionic conductivity, spectroscopy, and computational studies on acidic ionic liquids are covered in the next sections. The final section provides a comprehensive review on applications of acidic ionic liquids in a wide array of fields including catalysis, CO2 fixation, ionogel, electrolyte, fuel-cell, membrane, biomass processing, biodiesel synthesis, desulfurization of gasoline/diesel, metal processing, and metal electrodeposition.

  17. [Biosynthesis of adipic acid].

    Science.gov (United States)

    Han, Li; Chen, Wujiu; Yuan, Fei; Zhang, Yuanyuan; Wang, Qinhong; Ma, Yanhe

    2013-10-01

    Adipic acid is a six-carbon dicarboxylic acid, mainly for the production of polymers such as nylon, chemical fiber and engineering plastics. Its annual demand is close to 3 million tons worldwide. Currently, the industrial production of adipic acid is based on the oxidation of aromatics from non-renewable petroleum resources by chemo-catalytic processes. It is heavily polluted and unsustainable, and the possible alternative method for adipic acid production should be developed. In the past years, with the development of synthetic biology and metabolic engineering, green and clean biotechnological methods for adipic acid production attracted more attention. In this study, the research advances of adipic acid and its precursor production are reviewed, followed by addressing the perspective of the possible new pathways for adipic acid production.

  18. Demospongic Acids Revisited

    Directory of Open Access Journals (Sweden)

    Gilles Barnathan

    2010-10-01

    Full Text Available The well-known fatty acids with a D5,9 unsaturation system were designated for a long period as demospongic acids, taking into account that they originally occurred in marine Demospongia sponges. However, such acids have also been observed in various marine sources with a large range of chain-lengths (C16–C32 and from some terrestrial plants with short acyl chains (C18–C19. Finally, the D5,9 fatty acids appear to be a particular type of non-methylene-interrupted fatty acids (NMA FAs. This article reviews the occurrence of these particular fatty acids in marine and terrestrial organisms and shows the biosynthetic connections between D5,9 fatty acids and other NMI FAs.

  19. Boric acid and boronic acids inhibition of pigeonpea urease.

    Science.gov (United States)

    Reddy, K Ravi Charan; Kayastha, Arvind M

    2006-08-01

    Urease from the seeds of pigeonpea was competitively inhibited by boric acid, butylboronic acid, phenylboronic acid, and 4-bromophenylboronic acid; 4-bromophenylboronic acid being the strongest inhibitor, followed by boric acid > butylboronic acid > phenylboronic acid, respectively. Urease inhibition by boric acid is maximal at acidic pH (5.0) and minimal at alkaline pH (10.0), i.e., the trigonal planar B(OH)3 form is a more effective inhibitor than the tetrahedral B(OH)4 -anionic form. Similarly, the anionic form of phenylboronic acid was least inhibiting in nature.

  20. Analgesic use - prevalence, biomonitoring and endocrine and reproductive effects

    DEFF Research Database (Denmark)

    Kristensen, David Møbjerg; Mazaud-Guittot, Sverine; Gaudriault, Pierre

    2016-01-01

    Paracetamol and NSAIDs, in particular acetylsalicylic acid (aspirin) and ibuprofen, are among the most used and environmentally released pharmaceutical drugs. The differences in international trends in the sale and consumption of mild analgesics reflect differences in marketing, governmental...... policies, habits, accessibility, disease patterns and the age distribution of each population. Biomonitoring indicates ubiquitous and high human exposure to paracetamol and to salicylic acid, which is the main metabolite of acetylsalicylic acid. Furthermore, evidence suggests that analgesics can have...

  1. Acid-Base Homeostasis.

    Science.gov (United States)

    Hamm, L Lee; Nakhoul, Nazih; Hering-Smith, Kathleen S

    2015-12-07

    Acid-base homeostasis and pH regulation are critical for both normal physiology and cell metabolism and function. The importance of this regulation is evidenced by a variety of physiologic derangements that occur when plasma pH is either high or low. The kidneys have the predominant role in regulating the systemic bicarbonate concentration and hence, the metabolic component of acid-base balance. This function of the kidneys has two components: reabsorption of virtually all of the filtered HCO3(-) and production of new bicarbonate to replace that consumed by normal or pathologic acids. This production or generation of new HCO3(-) is done by net acid excretion. Under normal conditions, approximately one-third to one-half of net acid excretion by the kidneys is in the form of titratable acid. The other one-half to two-thirds is the excretion of ammonium. The capacity to excrete ammonium under conditions of acid loads is quantitatively much greater than the capacity to increase titratable acid. Multiple, often redundant pathways and processes exist to regulate these renal functions. Derangements in acid-base homeostasis, however, are common in clinical medicine and can often be related to the systems involved in acid-base transport in the kidneys.

  2. Bile acid sequestrants

    DEFF Research Database (Denmark)

    Hansen, Morten; Sonne, David P; Knop, Filip K

    2014-01-01

    Bile acids are synthesized in the liver from cholesterol and have traditionally been recognized for their role in absorption of lipids and in cholesterol homeostasis. In recent years, however, bile acids have emerged as metabolic signaling molecules that are involved in the regulation of lipid...... and glucose metabolism, and possibly energy homeostasis, through activation of the bile acid receptors farnesoid X receptor (FXR) and TGR5. Bile acid sequestrants (BASs) constitute a class of drugs that bind bile acids in the intestine to form a nonabsorbable complex resulting in interruption...... of the enterohepatic circulation. This increases bile acid synthesis and consequently reduces serum low-density lipoprotein cholesterol. Also, BASs improve glycemic control in patients with type 2 diabetes. Despite a growing understanding of the impact of BASs on glucose metabolism, the mechanisms behind their glucose...

  3. Citric Acid Alternative to Nitric Acid Passivation

    Science.gov (United States)

    Lewis, Pattie L. (Compiler)

    2013-01-01

    The Ground Systems Development and Operations GSDO) Program at NASA John F. Kennedy Space Center (KSC) has the primary objective of modernizing and transforming the launch and range complex at KSC to benefit current and future NASA programs along with other emerging users. Described as the launch support and infrastructure modernization program in the NASA Authorization Act of 2010, the GSDO Program will develop and implement shared infrastructure and process improvements to provide more flexible, affordable, and responsive capabilities to a multi-user community. In support of the GSDO Program, the purpose of this project is to demonstratevalidate citric acid as a passivation agent for stainless steel. Successful completion of this project will result in citric acid being qualified for use as an environmentally preferable alternative to nitric acid for passivation of stainless steel alloys in NASA and DoD applications.

  4. Parenteral Nutrition: Amino Acids

    Science.gov (United States)

    Hoffer, Leonard John

    2017-01-01

    There is growing interest in nutrition therapies that deliver a generous amount of protein, but not a toxic amount of energy, to protein-catabolic critically ill patients. Parenteral amino acids can achieve this goal. This article summarizes the biochemical and nutritional principles that guide parenteral amino acid therapy, explains how parenteral amino acid solutions are formulated, and compares the advantages and disadvantages of different parenteral amino acid products with enterally-delivered whole protein products in the context of protein-catabolic critical illness. PMID:28287411

  5. Parenteral Nutrition: Amino Acids.

    Science.gov (United States)

    Hoffer, Leonard John

    2017-03-10

    There is growing interest in nutrition therapies that deliver a generous amount of protein, but not a toxic amount of energy, to protein-catabolic critically ill patients. Parenteral amino acids can achieve this goal. This article summarizes the biochemical and nutritional principles that guide parenteral amino acid therapy, explains how parenteral amino acid solutions are formulated, and compares the advantages and disadvantages of different parenteral amino acid products with enterally-delivered whole protein products in the context of protein-catabolic critical illness.

  6. Diterpenoid acids from Grindelia nana.

    Science.gov (United States)

    Mahmoud, A A; Ahmed, A A; Tanaka, T; Iinuma, M

    2000-03-01

    Two new norditerpenoid acids of the labdane-type (norgrindelic acids), 4,5-dehydro-6-oxo-18-norgrindelic acid (1) and 4beta-hydroxy-6-oxo-19-norgrindelic acid (2), as well as a new grindelic acid derivative, 18-hydroxy-6-oxogrindelic acid (3), were isolated from the aerial parts of Grindelia nana. In addition, the known compounds, 6-oxogrindelic acid, grindelic acid, methyl grindeloate, 7alpha,8alpha-epoxygrindelic acid, and 4alpha-carboxygrindelic acid were also isolated. The structures of the new compounds were characterized on the basis of spectroscopic analysis.

  7. Hemarthrosis of the knees following streptokinase therapy for acute myocardial infarction

    OpenAIRE

    Pimenta Eduardo; Anti Sônia M. A.

    2003-01-01

    A sixty-four-year-old male patient was studied who had acute coronary syndrome with ST segment elevation experienced bilateral hemarthrosis of the knees after administration of streptokinase and acetylsalicylic acid.

  8. Aspirin-Induced Neonatal Intracranial Hemorrhage

    OpenAIRE

    1994-01-01

    A term newborn infant with intracranial hemorrhage associated with maternal acetylsalicylic acid ingestion before delivery is reported from the Departments of Pediatrics and Neurology, Eastern Virginia Medical School, Norfolk, VA.

  9. Nonsteroidal Anti-Inflammatory Drugs: Adverse Effects and Their Prevention

    NARCIS (Netherlands)

    Vonkeman, Harald E.; Laar, van de Mart A.F.J.

    2010-01-01

    Objectives: To discuss nonsteroidal anti-inflammatory drugs (NSAIDs), their history, development, mode of action, toxicities, strategies for the prevention of toxicity, and future developments. - Methods: Medline search for articles published up to 2007, using the keywords acetylsalicylic acid, asp

  10. Influence of genetic variants and drug interactions on the response to antiplatelet drugs

    NARCIS (Netherlands)

    Harmsze, A.M.

    2011-01-01

    Antiplatelet therapy plays an important role in the treatment of cardiovascular disease. The combination of acetylsalicylic acid and clopidogrel is routine care in patients with acute coronary syndromes (ACS) or undergoing percutaneous coronary interventions (PCI). Although the effectiveness of anti

  11. Blødningskomplikationer ved behandling med clopidogrel og acetylsalicylsyre efter akut koronart syndrom

    DEFF Research Database (Denmark)

    Kjær, Janus; Larsen, Christian Hastrup; Poulsen, Tina Svenstrup

    2006-01-01

    INTRODUCTION: The Clopidogrel in Unstable Angina to Prevent Recurrent Events (CURE) study showed that patients with unstable angina pectoris (UAP) and non-ST-elevation myocardial infarction (NSTEMI) benefit from combined therapy with acetylsalicylic acid (ASA) and clopidogrel. However, only...

  12. Spontaneous reports on drug-induced pancreatitis in Denmark from 1968 to 1999

    DEFF Research Database (Denmark)

    Andersen, V; Sonne, J; Andersen, M

    2001-01-01

    -acetylsalicylic acid agents, angiotensin-converting enzyme inhibitors, estrogen preparations, didanosine, valproate, codeine, antiviral agents used in acquired immunodeficiency syndrome therapy, various lipid-reducing agents, interferon, paracetamol, griseofulvin, ticlopine, allopurinol, lithium and the MMR...

  13. Hemarthrosis of the knees following streptokinase therapy for acute myocardial infarction

    Directory of Open Access Journals (Sweden)

    Pimenta Eduardo

    2003-01-01

    Full Text Available A sixty-four-year-old male patient was studied who had acute coronary syndrome with ST segment elevation experienced bilateral hemarthrosis of the knees after administration of streptokinase and acetylsalicylic acid.

  14. Topical Acne Treatments and Pregnancy

    Science.gov (United States)

    ... may be concern when a pregnant woman takes acetylsalicylic acid (aspirin), a related medication which is taken by mouth. At doses used for pain relief, aspirin has been shown to interfere with the development ...

  15. Amino Acid Crossword Puzzle

    Science.gov (United States)

    Sims, Paul A.

    2011-01-01

    Learning the 20 standard amino acids is an essential component of an introductory course in biochemistry. Later in the course, the students study metabolism and learn about various catabolic and anabolic pathways involving amino acids. Learning new material or concepts often is easier if one can connect the new material to what one already knows;…

  16. Peptide Nucleic Acids (PNA)

    DEFF Research Database (Denmark)

    2002-01-01

    A novel class of compounds, known as peptide nucleic acids, bind complementary ssDNA and RNA strands more strongly than a corresponding DNA. The peptide nucleic acids generally comprise ligands such as naturally occurring DNA bases attached to a peptide backbone through a suitable linker....

  17. Peptide Nucleic Acids

    DEFF Research Database (Denmark)

    1998-01-01

    A novel class of compounds, known as peptide nucleic acids, bind complementary ssDNA and RNA strands more strongly than a corresponding DNA. The peptide nucleic acids generally comprise ligands such as naturally occurring DNA bases attached to a peptide backbone through a suitable linker....

  18. Peptide Nucleic Acids

    DEFF Research Database (Denmark)

    2003-01-01

    A novel class of compounds, known as peptide nucleic acids, bind complementary ssDNA and RNA strands more strongly than a corresponding DNA. The peptide nucleic acids generally comprise ligands such as naturally occurring DNA bases attached to a peptide backbone through a suitable linker....

  19. Peptide Nucleic Acids

    DEFF Research Database (Denmark)

    2004-01-01

    A novel class of compounds known as peptide nucleic acids, bind complementary DNA and RNA strands, and generally do so more strongly than the corresponding DNA or RNA strands while exhibiting increased sequence specificity and solubility. The peptide nucleic acids comprise ligands selected from...

  20. Carbolic acid poisoning

    Science.gov (United States)

    ... you to. If the person swallowed the carbolic acid, give them water or milk right away, if a provider tells ... well someone does depends on how much carbolic acid they swallowed and how quickly they receive treatment. The faster medical help is given, the better ...

  1. Fats and fatty acids

    Science.gov (United States)

    The absolute fat requirement of the human species is the amount of essential fatty acids needed to maintain optimal fatty acid composition of all tissues and normal eicosanoid synthesis. At most, this requirement is no more than about 5% of an adequate energy intake. However, fat accounts for appro...

  2. Locked nucleic acid

    DEFF Research Database (Denmark)

    Jepsen, Jan Stenvang; Sørensen, Mads D; Wengel, Jesper

    2004-01-01

    Locked nucleic acid (LNA) is a class of nucleic acid analogs possessing very high affinity and excellent specificity toward complementary DNA and RNA, and LNA oligonucleotides have been applied as antisense molecules both in vitro and in vivo. In this review, we briefly describe the basic...

  3. Peptide Nucleic Acid Synthons

    DEFF Research Database (Denmark)

    2004-01-01

    A novel class of compounds, known as peptide nucleic acids, bind complementary ssDNA and RNA strands more strongly than a corresponding DNA. The peptide nucleic acids generally comprise ligands such as naturally occurring DNA bases attached to a peptide backbone through a suitable linker....

  4. Chlorogenic acid and caffeic acid are absorbed in humans

    OpenAIRE

    2001-01-01

    Chlorogenic acid, an ester of caffeic acid and quinic acid, is a major phenolic compound in coffee; daily intake in coffee drinkers is 0.5-1 g. Chlorogenic acid and caffeic acid are antioxidants in vitro and might therefore contribute to the prevention of cardiovascular disease. However, data on the absorption of chlorogenic acid and caffeic acid in humans are lacking. We determined the absorption of chlorogenic acid and caffeic acid in a cross-over study with 4 female and 3 male healthy ileo...

  5. Chlorogenic acid and caffeic acid are absorbed in humans

    NARCIS (Netherlands)

    Olthof, M.R.; Hollman, P.C.H.; Katan, M.B.

    2001-01-01

    Chlorogenic acid, an ester of caffeic acid and quinic acid, is a major phenolic compound in coffee; daily intake in coffee drinkers is 0.5-1 g. Chlorogenic acid and caffeic acid are antioxidants in vitro and might therefore contribute to the prevention of cardiovascular disease. However, data on the

  6. 2-Methylaspartic acid monohydrate

    Directory of Open Access Journals (Sweden)

    Ray J. Butcher

    2013-12-01

    Full Text Available The title compound, C5H9NO4·H2O, is an isomer of the α-amino acid glutamic acid that crystallizes from water in its zwitterionic form as a monohydrate. It is not one of the 20 proteinogenic α-amino acids that are used in living systems and differs from the natural amino acids in that it has an α-methyl group rather than an α-H atom. In the crystal, an O—H...O hydrogen bond is present between the acid and water molecules while extensive N—H...O and O—H...O hydrogen bonds link the components into a three-dimensional array.

  7. Halogenated fatty acids

    DEFF Research Database (Denmark)

    Mu, Huiling; Wesén, Clas; Sundin, Peter

    1997-01-01

    Chlorinated fatty acids have been found to be major contributors to organohalogen compounds in fish, bivalves, jellyfish, and lobster, and they have been indicated to contribute considerably to organohalogens in marine mammals. Brominated fatty acids have been found in marine sponges. Also......, chlorinated lipids have been found in meat exposed to hypochlorite disinfected water, and in chlorine-treated flour and in products made from such flour. Following exposure to chlorine bleached pulp mill effluents, aquatic organisms may have elevated concentrations of chlorinated fatty acids in their lipids....... However, a natural production of halogenated fatty acids is also possible. In this paper we summarize the present knowledge of the occurrence of halogenated fatty acids in lipids and suggested ways of their formation. In Part II (Trends Anal. Chem. 16 (1997) 274) we deal with methods...

  8. Fusidic acid in dermatology

    DEFF Research Database (Denmark)

    Schöfer, Helmut; Simonsen, Lene

    1995-01-01

    Studies on the clinical efficacy of fusidic acid in skin and soft-tissue infections (SSTIs), notably those due to Staphylococcus aureus, are reviewed. Oral fusidic acid (tablets dosed at 250 mg twice daily, or a suspension for paediatric use at 20 mg/kg/day given as two daily doses) has shown good...... efficacy and tolerability. Similarly, plain fusidic acid cream or ointment used two or three times daily in SSTIs such as impetigo are clinically and bacteriologically effective, with minimal adverse events. Combination formulations of fusidic acid with 1% hydrocortisone or 0.1% betamethasone achieve...... excellent results in infected eczema by addressing both inflammation and infection. A new lipid-rich combination formulation provides an extra moisturizing effect. Development of resistance to fusidic acid has remained generally low or short-lived and can be minimized by restricting therapy to no more than...

  9. 21 CFR 172.860 - Fatty acids.

    Science.gov (United States)

    2010-04-01

    ... acid, caprylic acid, lauric acid, myristic acid, oleic acid, palmitic acid, and stearic acid. (b) The... 21 Food and Drugs 3 2010-04-01 2009-04-01 true Fatty acids. 172.860 Section 172.860 Food and Drugs... Multipurpose Additives § 172.860 Fatty acids. The food additive fatty acids may be safely used in food and...

  10. Gluconic acid production.

    Science.gov (United States)

    Anastassiadis, Savas; Morgunov, Igor G

    2007-01-01

    Gluconic acid, the oxidation product of glucose, is a mild neither caustic nor corrosive, non toxic and readily biodegradable organic acid of great interest for many applications. As a multifunctional carbonic acid belonging to the bulk chemicals and due to its physiological and chemical characteristics, gluconic acid itself, its salts (e.g. alkali metal salts, in especially sodium gluconate) and the gluconolactone form have found extensively versatile uses in the chemical, pharmaceutical, food, construction and other industries. Present review article presents the comprehensive information of patent bibliography for the production of gluconic acid and compares the advantages and disadvantages of known processes. Numerous manufacturing processes are described in the international bibliography and patent literature of the last 100 years for the production of gluconic acid from glucose, including chemical and electrochemical catalysis, enzymatic biocatalysis by free or immobilized enzymes in specialized enzyme bioreactors as well as discontinuous and continuous fermentation processes using free growing or immobilized cells of various microorganisms, including bacteria, yeast-like fungi and fungi. Alternatively, new superior fermentation processes have been developed and extensively described for the continuous and discontinuous production of gluconic acid by isolated strains of yeast-like mold Aureobasidium pullulans, offering numerous advantages over the traditional discontinuous fungi processes.

  11. Trans Fatty Acids

    Science.gov (United States)

    Doyle, Ellin

    1997-09-01

    Fats and their various fatty acid components seem to be a perennial concern of nutritionists and persons concerned with healthful diets. Advice on the consumption of saturated, polyunsaturated, monounsaturated, and total fat bombards us from magazines and newspapers. One of the newer players in this field is the group of trans fatty acids found predominantly in partially hydrogenated fats such as margarines and cooking fats. The controversy concerning dietary trans fatty acids was recently addressed in an American Heart Association (AHA) science advisory (1) and in a position paper from the American Society of Clinical Nutrition/American Institute of Nutrition (ASCN/AIN) (2). Both reports emphasize that the best preventive strategy for reducing risk for cardiovascular disease and some types of cancer is a reduction in total and saturated fats in the diet, but a reduction in the intake of trans fatty acids was also recommended. Although the actual health effects of trans fatty acids remain uncertain, experimental evidence indicates that consumption of trans fatty acids adversely affects serum lipid levels. Since elevated levels of serum cholesterol and triacylglycerols are associated with increased risk of cardiovascular disease, it follows that intake of trans fatty acids should be minimized.

  12. Amino acid racemisation dating

    Energy Technology Data Exchange (ETDEWEB)

    Murray-Wallace, C.V. [University of Wollongong, Wollongong, NSW (Australia). School of Geosciences

    1999-11-01

    The potential of the time-dependent amino acid racemisation reaction as a method of age assessment was first reported by Hare and Abelson (1968). They noted that in specimens of the bivalve mollusc Mercenaria sp., greater concentrations of amino acids in the D-configuration with increasing fossil age. Hare and Abelson (1968) also reported negligible racemisation in a modern specimen of Mecanaria sp. On this basis they suggested that the extent of amino acid racemisation (epimerisation in the case of isoleucine) may be used to assess the age of materials within and beyond the range of radiocarbon dating. For the past thirty years amino acid racemisation has been extensively applied in Quaternary research as a method of relative and numeric dating, and a particularly large literature has emerged on the subject 12 refs.

  13. [Hydrofluoric acid burns].

    Science.gov (United States)

    Holla, Robin; Gorter, Ramon R; Tenhagen, Mark; Vloemans, A F P M Jos; Breederveld, Roelf S

    2016-01-01

    Hydrofluoric acid is increasingly used as a rust remover and detergent. Dermal contact with hydrofluoric acid results in a chemical burn characterized by severe pain and deep tissue necrosis. It may cause electrolyte imbalances with lethal consequences. It is important to identify high-risk patients. 'High risk' is defined as a total affected body area > 3% or exposure to hydrofluoric acid in a concentration > 50%. We present the cases of three male patients (26, 31, and 39 years old) with hydrofluoric acid burns of varying severity and describe the subsequent treatments. The application of calcium gluconate 2.5% gel to the skin is the cornerstone of the treatment, reducing pain as well as improving wound healing. Nails should be thoroughly inspected and possibly removed if the nail is involved, to ensure proper healing. In high-risk patients, plasma calcium levels should be evaluated and cardiac monitoring is indicated.

  14. Acid rain: An overview

    Data.gov (United States)

    US Fish and Wildlife Service, Department of the Interior — Summary of the effects of acid rain and related processes, sources, issues, corrective actions, research, current law, potential solutions, political solutions,...

  15. Folic acid - test

    Science.gov (United States)

    ... folic acid before and during pregnancy helps prevent neural tube defects, such as spina bifida. Women who are ... take more if they have a history of neural tube defects in earlier pregnancies. Ask your provider how ...

  16. Stomach acid test

    Science.gov (United States)

    Gastric acid secretion test ... The test is done after you have not eaten for a while so fluid is all that remains in ... injected into your body. This is done to test the ability of the cells in the stomach ...

  17. Fatty Acid Oxidation Disorders

    Science.gov (United States)

    ... acid oxidation disorders are tested for in newborn screening? The March of Dimes recommends that all babies ... in behavior Diarrhea, nausea (feeling sick to your stomach) and throwing up Drowsiness Fever Fussiness Little appetite ...

  18. Amino Acids and Chirality

    Science.gov (United States)

    Cook, Jamie E.

    2012-01-01

    Amino acids are among the most heavily studied organic compound class in carbonaceous chondrites. The abundance, distributions, enantiomeric compositions, and stable isotopic ratios of amino acids have been determined in carbonaceous chondrites fi'om a range of classes and petrographic types, with interesting correlations observed between these properties and the class and typc of the chondritcs. In particular, isomeric distributions appear to correlate with parent bodies (chondrite class). In addition, certain chiral amino acids are found in enantiomeric excess in some chondrites. The delivery of these enantiomeric excesses to the early Earth may have contributed to the origin of the homochirality that is central to life on Earth today. This talk will explore the amino acids in carbonaceous chondritcs and their relevance to the origin of life.

  19. 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...

  20. Neutron Nucleic Acid Crystallography.

    Science.gov (United States)

    Chatake, Toshiyuki

    2016-01-01

    The hydration shells surrounding nucleic acids and hydrogen-bonding networks involving water molecules and nucleic acids are essential interactions for the structural stability and function of nucleic acids. Water molecules in the hydration shells influence various conformations of DNA and RNA by specific hydrogen-bonding networks, which often contribute to the chemical reactivity and molecular recognition of nucleic acids. However, X-ray crystallography could not provide a complete description of structural information with respect to hydrogen bonds. Indeed, X-ray crystallography is a powerful tool for determining the locations of water molecules, i.e., the location of the oxygen atom of H2O; however, it is very difficult to determine the orientation of the water molecules, i.e., the orientation of the two hydrogen atoms of H2O, because X-ray scattering from the hydrogen atom is very small.Neutron crystallography is a specialized tool for determining the positions of hydrogen atoms. Neutrons are not diffracted by electrons, but are diffracted by atomic nuclei; accordingly, neutron scattering lengths of hydrogen and its isotopes are comparable to those of non-hydrogen atoms. Therefore, neutron crystallography can determine both of the locations and orientations of water molecules. This chapter describes the current status of neutron nucleic acid crystallographic research as well as the basic principles of neutron diffraction experiments performed on nucleic acid crystals: materials, crystallization, diffraction experiments, and structure determination.

  1. Fatty Acid Biosynthesis IX

    DEFF Research Database (Denmark)

    Carey, E. M.; Hansen, Heinz Johs. Max; Dils, R.

    1972-01-01

    # 1. I. [I-14C]Acetate was covalently bound to rabbit mammary gland fatty acid synthetase by enzymic transacylation from [I-14C]acetyl-CoA. Per mole of enzyme 2 moles of acetate were bound to thiol groups and up to I mole of acetate was bound to non-thiol groups. # 2. 2. The acetyl-fatty acid...... synthetase complex was isolated free from acetyl-CoA. It was rapidly hydrolysed at 30°C, but hydrolysis was greatly diminished at o°C and triacetic lactone synthesis occurred. In the presence of malonyl-CoA and NADPH, all the acetate bound to fatty acid synthetase was incorporated into long-chain fatty acids....... Hydrolysis of bound acetate and incorporation of bound acetate into fatty acids were inhibited to the same extent by guanidine hydrochloride. # 3. 3. Acetate was also covalently bound to fatty acid synthetase by chemical acetylation with [I-14C]acetic anhydride in the absence of CoASH. A total of 60 moles...

  2. Performance Comparison of New Combinations of Acids with Mud Acid in Sandstone Acidizing

    Directory of Open Access Journals (Sweden)

    Mian Umer Shafiq

    2014-01-01

    Full Text Available The aim of this research is to find the best suitable acid to acidize undamaged low permeable sandstone formation Stimulation of sandstone formations is a challenging task, which involves several chemicals and physical interactions of the acid with the formation. Mud acid has been successfully used to stimulate sandstone reservoirs for a number of years. Matrix acidizing may also be used to increase formation permeability in undamaged wells. The change may be up to 50 to 100% with the mud acid. For any acidizing process, the selection of acid (Formulation and Concentration and the design (Pre-flush, Main Acid, After-flush is very important. Different researchers are using different combinations of acids with different concentrations to get the best results for acidization. Mainly the common practice is combination of Hydrochloric Acid- Hydrofluoric with Concentration (3% HF-12% HCl. This study presents the results of a laboratory investigation of Orthophosphoric acid instead of hydrochloric acid in one combination and the second combination is Fluoboric and formic acid and the third one is formic and hydrofluoric acid. The results are compared with the mud acid and the results analyzed are porosity, permeability, strength, color change and FESEM Analysis. All of these new combinations shows that these have the potential to be used as acidizing acids on sandstone formations.

  3. Inhibitory effect of ethanol, acetic acid, propionic acid and butyric acid on fermentative hydrogen production

    Energy Technology Data Exchange (ETDEWEB)

    Wang, Bo; Wan, Wei; Wang, Jianlong [Laboratory of Environmental Technology, INET, Tsinghua University, Beijing 100084 (China)

    2008-12-15

    The inhibitory effect of added ethanol, acetic acid, propionic acid and butyric acid on fermentative hydrogen production by mixed cultures was investigated in batch tests using glucose as substrate. The experimental results showed that, at 35 C and initial pH 7.0, during the fermentative hydrogen production, the substrate degradation efficiency, hydrogen production potential, hydrogen yield and hydrogen production rate all trended to decrease with increasing added ethanol, acetic acid, propionic acid and butyric acid concentration from 0 to 300 mmol/L. The inhibitory effect of added ethanol on fermentative hydrogen production was smaller than those of added acetic acid, propionic acid and butyric acid. The modified Han-Levenspiel model could describe the inhibitory effects of added ethanol, acetic acid, propionic acid and butyric acid on fermentative hydrogen production rate in this study successfully. The modified Logistic model could describe the progress of cumulative hydrogen production. (author)

  4. Amino acids in the sedimentary humic and fulvic acids

    Digital Repository Service at National Institute of Oceanography (India)

    Sardessai, S.

    Humic and fulvic acids isolated from a few sediment samples from Arabian Sea and Bay of Bengal were analysed for total hydrolysable amino acids concentration and their composition. The amono acids content of fulvic acids was higher than in the humic...

  5. Synthesis and anticonvulsant activity of novel bicyclic acidic amino acids

    DEFF Research Database (Denmark)

    Conti, Paola; De Amici, Marco; Joppolo Di Ventimiglia, Samuele

    2003-01-01

    Bicyclic acidic amino acids (+/-)-6 and (+/-)-7, which are conformationally constrained homologues of glutamic acid, were prepared via a strategy based on a 1,3-dipolar cycloaddition. The new amino acids were tested toward ionotropic and metabotropic glutamate receptor subtypes; both of them...

  6. EFFECT OF ACIDITY ON ACID-SENSITIVE UV CURING SYSTEM

    Institute of Scientific and Technical Information of China (English)

    Qi-dao Chen; Bing Wu; Xiao-yin Hong

    1999-01-01

    By using diphenyliodonium salts with different counterions as photo acid generators (PAGs), the effect of acidity on ring-opening polymerization of epoxy monomers and polycondensation of polyol with hexamethoxymethyl melamine (HMMM) was studied. The result shows that the rate of ring-opening polymerization is evidently dependent on the acidity of the acid and strong photo-generated acid is required.However, there is a leveling effect in the polycondensation system; if the photo-generated acid is stronger than protonated HMMM, the acidity does not obviously affect the polycondensation rate.

  7. Determination of Sialic Acids by Acidic Ninhydrin Reaction

    Directory of Open Access Journals (Sweden)

    Yao,Kenzabroh

    1987-12-01

    Full Text Available A new acidic ninhydrin method for determining free sialic acids is described. The method is based on the reaction of sialic acids with Gaitonde's acid ninhydrin reagent 2 which yields a stable color with an absorption maximum at 470 nm. The standard curve is linear in the range of 5 to 500 nmol of N-acetylneuraminic acid per 0.9 ml of reaction mixture. The reaction was specific only for sialic acids among the various sugars and sugar derivatives examined. Some interference of this method by cysteine, cystine and tryptophan was noted, although their absorption maxima differed from that of sialic acids. The interference by these amino acids was eliminated with the use of a small column of cation-exchange resin. The acidic ninhydrin method provides a simple and rapid method for the determination of free sialic acids in biological materials.

  8. Domoic Acid Epileptic Disease

    Directory of Open Access Journals (Sweden)

    John S. Ramsdell

    2014-03-01

    Full Text Available Domoic acid epileptic disease is characterized by spontaneous recurrent seizures weeks to months after domoic acid exposure. The potential for this disease was first recognized in a human case study of temporal lobe epilepsy after the 1987 amnesic shellfish-poisoning event in Quebec, and was characterized as a chronic epileptic syndrome in California sea lions through investigation of a series of domoic acid poisoning cases between 1998 and 2006. The sea lion study provided a breadth of insight into clinical presentations, unusual behaviors, brain pathology, and epidemiology. A rat model that replicates key observations of the chronic epileptic syndrome in sea lions has been applied to identify the progression of the epileptic disease state, its relationship to behavioral manifestations, and to define the neural systems involved in these behavioral disorders. Here, we present the concept of domoic acid epileptic disease as a delayed manifestation of domoic acid poisoning and review the state of knowledge for this disease state in affected humans and sea lions. We discuss causative mechanisms and neural underpinnings of disease maturation revealed by the rat model to present the concept for olfactory origin of an epileptic disease; triggered in dendodendritic synapases of the olfactory bulb and maturing in the olfactory cortex. We conclude with updated information on populations at risk, medical diagnosis, treatment, and prognosis.

  9. Hydrogen production by fermentation using acetic acid and lactic acid.

    Science.gov (United States)

    Matsumoto, Mitsufumi; Nishimura, Yasuhiko

    2007-03-01

    Microbial hydrogen production from sho-chu post-distillation slurry solution (slurry solution) containing large amounts of organic acids was investigated. The highest hydrogen producer, Clostridium diolis JPCC H-3, was isolated from natural environment and produced hydrogen at 6.03+/-0.15 ml from 5 ml slurry solution in 30 h. Interestingly, the concentration of acetic acid and lactic acid in the slurry solution decreased during hydrogen production. The substrates for hydrogen production by C. diolis JPCC H-3, in particular organic acids, were investigated in an artificial medium. No hydrogen was produced from acetic acid, propionic acid, succinic acid, or citric acid on their own. Hydrogen and butyric acid were produced from a mixture of acetic acid and lactic acid, showing that C. diolis. JPCC H-3 could produce hydrogen from acetic acid and lactic acid. Furthermore, calculation of the Gibbs free energy strongly suggests that this reaction would proceed. In this paper, we describe for the first time microbial hydrogen production from acetic acid and lactic acid by fermentation.

  10. Halogenated fatty acids

    DEFF Research Database (Denmark)

    Mu, Huiling; Sundin, Peter; Wesén, Clas

    1997-01-01

    Halogenated fatty acids are the major contributors to organohalogen compounds in lipids of marine mammals, fish, and bivalves. For the initial characterization of these recently noticed compounds, a determination of the halogen concentration has usually been combined with some lipid isolation...... and separation method. This review covers separation by solid phase chromatography, gel permeation chromatography, and liquid-liquid extraction, followed by halogen determination. All studies performed according to this outline have indicated that the major organohalogen compounds are chlorinated fatty acids...... bound in different lipids. For the detection and identification of individual, halogenated fatty acid methyl esters (FAMEs) liberated from the lipids, gas chromatography (GC) has been employed together with detection methods such as electron capture detection, electrolytic conductivity detection (ELCD...

  11. Calorimetry of Nucleic Acids.

    Science.gov (United States)

    Rozners, Eriks; Pilch, Daniel S; Egli, Martin

    2015-12-01

    This unit describes the application of calorimetry to characterize the thermodynamics of nucleic acids, specifically, the two major calorimetric methodologies that are currently employed: differential scanning (DSC) and isothermal titration calorimetry (ITC). DSC is used to study thermally induced order-disorder transitions in nucleic acids. A DSC instrument measures, as a function of temperature (T), the excess heat capacity (C(p)(ex)) of a nucleic acid solution relative to the same amount of buffer solution. From a single curve of C(p)(ex) versus T, one can derive the following information: the transition enthalpy (ΔH), entropy (ΔS), free energy (ΔG), and heat capacity (ΔCp); the state of the transition (two-state versus multistate); and the average size of the molecule that melts as a single thermodynamic entity (e.g., the duplex). ITC is used to study the hybridization of nucleic acid molecules at constant temperature. In an ITC experiment, small aliquots of a titrant nucleic acid solution (strand 1) are added to an analyte nucleic acid solution (strand 2), and the released heat is monitored. ITC yields the stoichiometry of the association reaction (n), the enthalpy of association (ΔH), the equilibrium association constant (K), and thus the free energy of association (ΔG). Once ΔH and ΔG are known, ΔS can also be derived. Repetition of the ITC experiment at a number of different temperatures yields the ΔCp for the association reaction from the temperature dependence of ΔH.

  12. 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.

  13. Whither Acid Rain?

    Directory of Open Access Journals (Sweden)

    Peter Brimblecombe

    2000-01-01

    Full Text Available Acid rain, the environmental cause célèbre of the 1980s seems to have vanished from popular conscience. By contrast, scientific research, despite funding difficulties, has continued to produce hundreds of research papers each year. Studies of acid rain taught much about precipitation chemistry, the behaviour of snow packs, long-range transport of pollutants and new issues in the biology of fish and forested ecosystems. There is now evidence of a shift away from research in precipitation and sulfur chemistry, but an impressive theoretical base remains as a legacy.

  14. Fatty acids of Thiobacillus thiooxidans.

    Science.gov (United States)

    Levin, R A

    1971-12-01

    Fatty acid spectra were made on Thiobacillus thiooxidans cultures both in the presence and absence of organic compounds. Small additions of glucose or acetate had no significant effect either on growth or fatty acid content. The addition of biotin had no stimulatory effect but did result in slight quantitative changes in the fatty acid spectrum. The predominant fatty acid was a C(19) cyclopropane acid.

  15. The Acid-Base Titration of a Very Weak Acid: Boric Acid

    Science.gov (United States)

    Celeste, M.; Azevedo, C.; Cavaleiro, Ana M. V.

    2012-01-01

    A laboratory experiment based on the titration of boric acid with strong base in the presence of d-mannitol is described. Boric acid is a very weak acid and direct titration with NaOH is not possible. An auxiliary reagent that contributes to the release of protons in a known stoichiometry facilitates the acid-base titration. Students obtain the…

  16. Lactic acid bacterial cell factories for gamma-aminobutyric acid.

    Science.gov (United States)

    Li, Haixing; Cao, Yusheng

    2010-11-01

    Gamma-aminobutyric acid is a non-protein amino acid that is widely present in organisms. Several important physiological functions of gamma-aminobutyric acid have been characterized, such as neurotransmission, induction of hypotension, diuretic effects, and tranquilizer effects. Many microorganisms can produce gamma-aminobutyric acid including bacteria, fungi and yeasts. Among them, gamma-aminobutyric acid-producing lactic acid bacteria have been a focus of research in recent years, because lactic acid bacteria possess special physiological activities and are generally regarded as safe. They have been extensively used in food industry. The production of lactic acid bacterial gamma-aminobutyric acid is safe and eco-friendly, and this provides the possibility of production of new naturally fermented health-oriented products enriched in gamma-aminobutyric acid. The gamma-aminobutyric acid-producing species of lactic acid bacteria and their isolation sources, the methods for screening of the strains and increasing their production, the enzymatic properties of glutamate decarboxylases and the relative fundamental research are reviewed in this article. And the potential applications of gamma-aminobutyric acid-producing lactic acid bacteria were also referred to.

  17. Effect of domoic acid on brain amino acid levels.

    Science.gov (United States)

    Durán, R; Arufe, M C; Arias, B; Alfonso, M

    1995-03-01

    The administration of Domoic Acid (Dom) in a 0.2 mg/kg i.p. dose induces changes in the levels of amino acids of neurochemical interest (Asp, Glu, Gly, Tau, Ala, GABA) in different rat brain regions (hypothalamus, hippocampus, amygdala, striatum, cortex and midbrain). The most affected amino acid is the GABA, the main inhibitory amino acid neurotransmitter, whereas glutamate, the main excitatory amino acid, is not affected. The rat brain regions that seem to be the main target of the Dom action belong to the limbic system (hippocampus, amygdala). The possible implication of the amino acids in the actions of Dom is also discussed.

  18. Koetjapic acid chloroform hemisolvate

    Directory of Open Access Journals (Sweden)

    Z. D. Nassar

    2010-06-01

    Full Text Available The asymmetric unit of the title compound, C30H46O4·0.5CHCl3, consists of one koetjapic acid [systematic name: (3R,4aR,4bS,7S,8S,10bS,12aS-7-(2-carboxyethyl-3,4b,7,10b,12a-pentamethyl-8-(prop-1-en-2-yl-1,2,3,4,4a,4b,5,6,7,8,9,10,10b,11,12,12a-hexadecahydrochrysene-3-carboxylic acid] molecule and one half-molecule of chloroform solvent, which is disordered about a twofold rotation axis. The symmetry-independent component is further disordered over two sites, with occupancies of 0.30 and 0.20. The koetjapic acid contains a fused four-ring system, A/B/C/D. The A/B, B/C and C/D junctions adopt E/trans/cis configurations, respectively. The conformation of ring A is intermediate between envelope and half-chair and ring B adopts an envelope conformation whereas rings C and D adopt chair conformations. A weak intramolecular C—H...O hydrogen bond is observed. The koetjapic acid molecules are linked into dimers by two pairs of intermolecular O—H...O hydrogen bonds. The dimers are stacked along the c axis.

  19. Phenylpyruvic acid in urine

    NARCIS (Netherlands)

    Meulemans, O.; Vergeer, E.G.

    1960-01-01

    The method of The, Fleury And Vink for the determination of phenylpyruvic acid (PPA) in urine is modified by measuring the extinction after the green colour with ferric chloride has faded, and subtracting this extinction from that found initially. More accurate values are obtained and low PPA values

  20. Accidents with sulfuric acid

    Directory of Open Access Journals (Sweden)

    Rajković Miloš B.

    2006-01-01

    Full Text Available Sulfuric acid is an important industrial and strategic raw material, the production of which is developing on all continents, in many factories in the world and with an annual production of over 160 million tons. On the other hand, the production, transport and usage are very dangerous and demand measures of precaution because the consequences could be catastrophic, and not only at the local level where the accident would happen. Accidents that have been publicly recorded during the last eighteen years (from 1988 till the beginning of 2006 are analyzed in this paper. It is very alarming data that, according to all the recorded accidents, over 1.6 million tons of sulfuric acid were exuded. Although water transport is the safest (only 16.38% of the total amount of accidents in that way 98.88% of the total amount of sulfuric acid was exuded into the environment. Human factor was the common factor in all the accidents, whether there was enough control of the production process, of reservoirs or transportation tanks or the transport was done by inadequate (old tanks, or the accidents arose from human factor (inadequate speed, lock of caution etc. The fact is that huge energy, sacrifice and courage were involved in the recovery from accidents where rescue teams and fire brigades showed great courage to prevent real environmental catastrophes and very often they lost their lives during the events. So, the phrase that sulfuric acid is a real "environmental bomb" has become clearer.

  1. Azetidinic amino acids

    DEFF Research Database (Denmark)

    Bräuner-Osborne, Hans; Bunch, Lennart; Chopin, Nathalie

    2005-01-01

    of two diastereoisomers that were easily separated and converted in two steps into azetidinic amino acids. Azetidines 35-44 were characterized in binding studies on native ionotropic Glu receptors and in functional assays at cloned metabotropic receptors mGluR1, 2 and 4, representing group I, II and III...

  2. Hyaluronic Acid Assays

    DEFF Research Database (Denmark)

    Itenov, Theis S; Kirkby, Nikolai S; Bestle, Morten H

    2015-01-01

    BACKGROUD: Hyaluronic acid (HA) is proposed as a marker of functional liver capacity. The aim of the present study was to compare a new turbidimetric assay for measuring HA with the current standard method. METHODS: HA was measured by a particle-enhanced turbidimetric immunoassay (PETIA) and enzyme...

  3. Lactic acid and lactates

    NARCIS (Netherlands)

    Schreurs, V.V.A.M.

    2010-01-01

    This review aims to integrate the present state of knowledge on lactate metabolism in human and mammalian physiology as far as it could be subject to nutritional interventions. An integrated view on the nutritional, metabolic and physiological aspects of lactic acid and lactates might open a perspec

  4. Acid Rain Investigations.

    Science.gov (United States)

    Hugo, John C.

    1992-01-01

    Presents an activity in which students investigate the formation of solid ammonium chloride aerosol particles to help students better understand the concept of acid rain. Provides activity objectives, procedures, sample data, clean-up instructions, and questions and answers to help interpret the data. (MDH)

  5. The Acid Rain Game.

    Science.gov (United States)

    Rakow, Steven J.; Glenn, Allen

    1982-01-01

    Provides rationale for and description of an acid rain game (designed for two players), a problem-solving model for elementary students. Although complete instructions are provided, including a copy of the game board, the game is also available for Apple II microcomputers. Information for the computer program is available from the author.…

  6. Acid Rain Classroom Projects.

    Science.gov (United States)

    Demchik, Michael J.

    2000-01-01

    Describes a curriculum plan in which students learn about acid rain through instructional media, research and class presentations, lab activities, simulations, design, and design implementation. Describes the simulation activity in detail and includes materials, procedures, instructions, examples, results, and discussion sections. (SAH)

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

    Energy Technology Data Exchange (ETDEWEB)

    Arceo, Elena; Ellman, Jonathan; Bergman, Robert

    2010-05-03

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

  8. Potentiometric determination of peroxodisulfuric acid during electrolysis sulfuric acid

    Directory of Open Access Journals (Sweden)

    Fedor Malchik

    2013-09-01

    Full Text Available Was proposed two potentiometric methods for determining peroxodisulfuric acid during electrolysis of sulfuric acid (potentiometric titration method and direct potentiometry, based on its interaction with a known excess of a solution Fe2+.

  9. Progress in engineering acid stress resistance of lactic acid bacteria.

    Science.gov (United States)

    Wu, Chongde; Huang, Jun; Zhou, Rongqing

    2014-02-01

    Lactic acid bacteria (LAB) are widely used for the production of a variety of fermented foods, and are considered as probiotic due to their health-promoting effect. However, LAB encounter various environmental stresses both in industrial fermentation and application, among which acid stress is one of the most important survival challenges. Improving the acid stress resistance may contribute to the application and function of probiotic action to the host. Recently, the advent of genomics, functional genomics and high-throughput technologies have allowed for the understanding of acid tolerance mechanisms at a systems level, and many method to improve acid tolerance have been developed. This review describes the current progress in engineering acid stress resistance of LAB. Special emphasis is placed on engineering cellular microenvironment (engineering amino acid metabolism, introduction of exogenous biosynthetic capacity, and overproduction of stress response proteins) and maintaining cell membrane functionality. Moreover, strategies to improve acid tolerance and the related physiological mechanisms are also discussed.

  10. Effect of phenolic acids on glucose and organic acid metabolism by lactic acid bacteria from wine.

    Science.gov (United States)

    Campos, Francisco M; Figueiredo, Ana R; Hogg, Tim A; Couto, José A

    2009-06-01

    The influence of phenolic (p-coumaric, caffeic, ferulic, gallic and protocatechuic) acids on glucose and organic acid metabolism by two strains of wine lactic acid bacteria (Oenococcus oeni VF and Lactobacillus hilgardii 5) was investigated. Cultures were grown in modified MRS medium supplemented with different phenolic acids. Cellular growth was monitored and metabolite concentrations were determined by HPLC-RI. Despite the strong inhibitory effect of most tested phenolic acids on the growth of O. oeni VF, the malolactic activity of this strain was not considerably affected by these compounds. While less affected in its growth, the capacity of L. hilgardii 5 to degrade malic acid was clearly diminished. Except for gallic acid, the addition of phenolic acids delayed the metabolism of glucose and citric acid in both strains tested. It was also found that the presence of hydroxycinnamic acids (p-coumaric, caffeic and ferulic) increased the yield of lactic and acetic acid production from glucose by O. oeni VF and not by L. hilgardii 5. The results show that important oenological characteristics of wine lactic acid bacteria, such as the malolactic activity and the production of volatile organic acids, may be differently affected by the presence of phenolic acids, depending on the bacterial species or strain.

  11. Circulating folic acid in plasma: relation to folic acid fortification

    Science.gov (United States)

    The implementation of folic acid fortification in the United States has resulted in unprecedented amounts of this synthetic form of folate in the American diet. Folic acid in circulation may be a useful measure of physiologic exposure to synthetic folic acid, and there is a potential for elevated co...

  12. Usnic acid controls the acidity tolerance of lichens.

    Science.gov (United States)

    Hauck, Markus; Jürgens, Sascha-René

    2008-11-01

    The hypotheses were tested that, firstly, lichens producing the dibenzofuran usnic acid colonize substrates characterized by specific pH ranges, secondly, this preferred pH is in a range where soluble usnic acid and its corresponding anion occur in similar concentrations, and thirdly, usnic acid makes lichens vulnerable to acidity. Lichens with usnic acid prefer an ambient pH range between 3.5 and 5.5 with an optimum between 4.0 and 4.5. This optimum is close to the pK(a1) value of usnic acid of 4.4. Below this optimum pH, dissolved SO(2) reduces the chlorophyll fluorescence yield more in lichens with than without their natural content of usnic acid. This suggests that usnic acid influences the acidity tolerance of lichens. The putative mechanism of the limited acidity tolerance of usnic acid-containing lichens is the acidification of the cytosol by molecules of protonated usnic acid shuttling protons through the plasma membrane at an apoplastic pH

  13. Acetic acid extraction from aqueous solutions using fatty acids

    NARCIS (Netherlands)

    IJmker, H.M.; Gramblicka, M.; Kersten, S.R.A.; Ham, van der A.G.J.; Schuur, B.

    2014-01-01

    A major challenge for production of acetic acid via bio-based routes is cost-effective concentration and purification of the acetic acid from the aqueous solutions, for which liquid–liquid extraction is a possible method. A main challenge in extraction of acetic acid from dilute aqueous solutions is

  14. Acid hydrolysis of cellulose

    Energy Technology Data Exchange (ETDEWEB)

    Salazar, H.

    1980-12-01

    One of the alternatives to increase world production of etha nol is by the hydrolysis of cellulose content of agricultural residues. Studies have been made on the types of hydrolysis: enzimatic and acid. Data obtained from the sulphuric acid hydrolysis of cellulose showed that this process proceed in two steps, with a yield of approximately 95% glucose. Because of increases in cost of alternatives resources, the high demand of the product and the more economic production of ethanol from cellulose materials, it is certain that this technology will be implemented in the future. At the same time further studies on the disposal and reuse of the by-products of this production must be undertaken.

  15. Autohydrolysis of phytic acid.

    Science.gov (United States)

    Hull, S R; Gray, J S; Montgomery, R

    1999-09-10

    The autohydrolysis of phytic acid at 120 degrees C resulted in the formation of most of the phosphate esters of myo-inositol in varying amounts depending upon the reaction time. Eighteen of the 39 chromatographically distinct myo-inositol mono-, bis-, tris-, tetrakis-, pentakis-, and hexakisphosphates have been characterized using two different HPLC systems. These myo-inositol phosphates were partially purified by preparative anion-exchange chromatography under acidic and alkaline elution conditions. The combination of these two methods provides a two-tiered chromatographic approach to the rapid and sensitive identification of inositol phosphates in complex mixtures. Identification of the products was confirmed by 1D and 2D (1)H NMR analysis. The analytical procedure was applied to the autohydrolysis of the mixture of inositol phosphates from corn steep water.

  16. N-(3-Methylphenylsuccinamic acid

    Directory of Open Access Journals (Sweden)

    B. Thimme Gowda

    2010-02-01

    Full Text Available In the crystal structure of the title compound, C11H13NO3, the conformations of the N—H and C=O bonds in the amide segment are anti to each other, and that of the amide H atom is anti to the meta-methyl group in the benzene ring. Furthermore, the conformations of the amide oxygen and the carbonyl O atom of the acid segment are also anti to the adjacent –CH2 groups. The C=O and O—H bonds of the acid group are syn to each other. In the crystal, the molecules are packed into infinite chains through intermolecular N—H...O and O—H...O hydrogen bonds.

  17. N-(3-Chlorophenylmaleamic acid

    Directory of Open Access Journals (Sweden)

    B. Thimme Gowda

    2010-07-01

    Full Text Available In the title compound, C10H8ClNO3, the molecular conformation is stabilized by two intramolecular hydrogen bonds. The first is a short O—H...O hydrogen bond within the maleamic acid unit and the second is a C—H...O hydrogen bond which connects the amide group with the phenyl ring. The maleamic acid unit is essentially planar, with an r.m.s. deviation of 0.044 Å, and makes a dihedral angle of 15.2 (1° with the phenyl ring. In the crystal, intermolecular N—H...O hydrogen bonds link the molecules into C(7 chains running [010].

  18. Accidents with sulfuric acid

    OpenAIRE

    Rajković Miloš B.

    2006-01-01

    Sulfuric acid is an important industrial and strategic raw material, the production of which is developing on all continents, in many factories in the world and with an annual production of over 160 million tons. On the other hand, the production, transport and usage are very dangerous and demand measures of precaution because the consequences could be catastrophic, and not only at the local level where the accident would happen. Accidents that have been publicly recorded during the last eigh...

  19. Phenolic acids bioavailability

    OpenAIRE

    2011-01-01

    The daily intake of phenolic compounds does not necessarily reflect the dose at which they reach the physiological targets in the organisms. The biological activity of phenolic compounds metabolites found in blood, organs and target tissues, as a result of digestive and hepatic activity, may differ from those of the native forms of the substances. This review discusses the absorption and metabolism of phenolic acids, a class of phenolic compounds abundant in food, and the methodologies used f...

  20. Omega-3 fatty acids (image)

    Science.gov (United States)

    Omega-3 fatty acids are a form of polyunsaturated fat that the body derives from food. Omega-3s (and omega-6s) are known as essential fatty acids (EFAs) because they are important for good health. ...

  1. Bile acids for viral hepatitis

    DEFF Research Database (Denmark)

    Chen, Weikeng; Liu, J; Gluud, C

    2007-01-01

    Trials have assessed bile acids for patients with viral hepatitis, but no consensus has been reached regarding their usefulness.......Trials have assessed bile acids for patients with viral hepatitis, but no consensus has been reached regarding their usefulness....

  2. LACTIC ACID BACTERIA: PROBIOTIC APPLICATIONS

    OpenAIRE

    NEENA GARG

    2015-01-01

    Lactic acid bacteria (LAB) is a heterotrophic Gram-positive bacteria which under goes lactic acid fermentations and leads to production of lactic acid as an end product. LAB includes Lactobacillus, Leuconostoc, Pediococcus, Lactococcus and Streptococcus which are grouped together in the family lactobacillaceae. LAB shows numerous antimicrobial activities due to production of antibacterial and antifungal compounds such as organic acids, bacteriocins, diacetyl, hydrogen peroxide and reutrin. LA...

  3. Biological properties of lipoic acid

    Directory of Open Access Journals (Sweden)

    Anna Bilska

    2002-06-01

    Full Text Available Lipoic acid is a prostetic group of H-protein of the glycine cleavage system and the dihydrolipoamide acyltransferases (E2 of the pyruvate, alpha-ketoglutarate and branched-chain alpha-keto acid dehydrogenase complexes. Lipoic acid and its reduced form, dihydrolipoic acid, reacts with oxygen reactive species. This paper reviews the beneficial effects in oxidative stress models or clinical conditions.

  4. Acids and bases solvent effects on acid-base strenght

    CERN Document Server

    Cox, Brian G

    2013-01-01

    Acids and bases are ubiquitous in chemistry. Our understanding of them, however, is dominated by their behaviour in water. Transfer to non-aqueous solvents leads to profound changes in acid-base strengths and to the rates and equilibria of many processes: for example, synthetic reactions involving acids, bases and nucleophiles; isolation of pharmaceutical actives through salt formation; formation of zwitter- ions in amino acids; and chromatographic separation of substrates. This book seeks to enhance our understanding of acids and bases by reviewing and analysing their behaviour in non-aqueous solvents. The behaviour is related where possible to that in water, but correlations and contrasts between solvents are also presented.

  5. Folic Acid: Data and Statistics

    Science.gov (United States)

    ... can prevent birth defects, or take vitamins containing folic acid before pregnancy. [ Read article ] Use of Supplements Containing Folic Acid ... Report has published a new study looking at folic acid use before pregnancy in women who have had a previous pregnancy ...

  6. Pantothenic acid biosynthesis in zymomonas

    Energy Technology Data Exchange (ETDEWEB)

    Tao, Luan; Tomb, Jean-Francois; Viitanen, Paul V.

    2014-07-01

    Zymomonas is unable to synthesize pantothenic acid and requires this essential vitamin in growth medium. Zymomonas strains transformed with an operon for expression of 2-dehydropantoate reductase and aspartate 1-decarboxylase were able to grow in medium lacking pantothenic acid. These strains may be used for ethanol production without pantothenic acid supplementation in seed culture and fermentation media.

  7. Acid Rain Limits Global Warming

    Institute of Scientific and Technical Information of China (English)

    Will Knight; 张林玲

    2004-01-01

    @@ Acid rain restricts global warming by reducing methane① emissions from natural wetland areas, suggests a global climate study. Acid rain is the result of industrial pollution,which causes rainwater to carry small quantities of acidic compoumds② such as sulphuric and nitric acid③. Contaminated rainwater can upset rivers and lakes, killing fish and other organisms and also damage plants, trees and buildings.

  8. Fumaric acid production by fermentation

    NARCIS (Netherlands)

    Roa Engel, C.A.; Straathof, A.J.J.; Zijlmans, T.W.; Van Gulik, W.M.; Van der Wielen, L.A.M.

    2008-01-01

    Abstract The potential of fumaric acid as a raw material in the polymer industry and the increment of cost of petroleum-based fumaric acid raises interest in fermentation processes for production of this compound from renewable resources. Although the chemical process yields 112% w/w fumaric acid fr

  9. Heterogeneous uptake of amines by citric acid and humic acid.

    Science.gov (United States)

    Liu, Yongchun; Ma, Qingxin; He, Hong

    2012-10-16

    Heterogeneous uptake of methylamine (MA), dimethylamine (DMA), and trimethylamine (TMA) onto citric acid and humic acid was investigated using a Knudsen cell reactor coupled to a quadrupole mass spectrometer at 298 K. Acid-base reactions between amines and carboxylic acids were confirmed. The observed uptake coefficients of MA, DMA, and TMA on citric acid at 298 K were measured to be 7.31 ± 1.13 × 10(-3), 6.65 ± 0.49 × 10(-3), and 5.82 ± 0.68 × 10(-3), respectively, and showed independence of sample mass. The observed uptake coefficients of MA, DMA, and TMA on humic acid at 298 K increased linearly with sample mass, and the true uptake coefficients of MA, DMA, and TMA were measured to be 1.26 ± 0.07 × 10(-5), 7.33 ± 0.40 × 10(-6), and 4.75 ± 0.15 × 10(-6), respectively. Citric acid, having stronger acidity, showed a higher reactivity than humic acid for a given amine; while the steric effect of amines was found to govern the reactivity between amines and citric acid or humic acid.

  10. Microbial degradation of poly(amino acid)s.

    Science.gov (United States)

    Obst, Martin; Steinbüchel, Alexander

    2004-01-01

    Natural poly(amino acid)s are a group of poly(ionic) molecules (ionomers) with various biological functions and putative technical applications and play, therefore, an important role both in nature and in human life. Because of their biocompatibility and their synthesis from renewable resources, poly(amino acid)s may be employed for many different purposes covering a broad spectrum of medical, pharmaceutical, and personal care applications as well as the domains of agriculture and of environmental applications. Biodegradability is one important advantage of naturally occurring poly(amino acid)s over many synthetic polymers. The intention of this review is to give an overview about the enzyme systems catalyzing the initial steps in poly(amino acid) degradation. The focus is on the naturally occurring poly(amino acid)s cyanophycin, poly(epsilon-L-lysine) and poly(gamma-glutamic acid); but biodegradation of structurally related synthetic polyamides such as poly(aspartic acid) and nylons, which are known from various technical applications, is also included.

  11. Molecular Interaction of Pinic Acid with Sulfuric Acid

    DEFF Research Database (Denmark)

    Elm, Jonas; Kurten, Theo; Bilde, Merete

    2014-01-01

    We investigate the molecular interactions between the semivolatile α-pinene oxidation product pinic acid and sulfuric acid using computational methods. The stepwise Gibbs free energies of formation have been calculated utilizing the M06-2X functional, and the stability of the clusters is evaluated...... from the corresponding ΔG values. The first two additions of sulfuric acid to pinic acid are found to be favorable with ΔG values of -9.06 and -10.41 kcal/mol. Addition of a third sulfuric acid molecule is less favorable and leads to a structural rearrangement forming a bridged sulfuric acid-pinic acid...... cluster. The involvement of more than one pinic acid molecule in a single cluster is observed to lead to the formation of favorable (pinic acid)2(H2SO4) and (pinic acid)2(H2SO4)2 clusters. The identified most favorable growth paths starting from a single pinic acid molecule lead to closed structures...

  12. Microbial transformations of isocupressic acid.

    Science.gov (United States)

    Lin, S J; Rosazza, J P

    1998-07-01

    Microbial transformations of the labdane-diterpene isocupressic acid (1) with different microorganisms yielded several oxygenated metabolites that were isolated and characterized by MS and NMR spectroscopic analyses. Nocardia aurantia (ATCC 12674) catalyzed the cleavage of the 13,14-double bond to yield a new nor-labdane metabolite, 2. Cunninghamella elegans (-) (NRRL 1393) gave 7beta-hydroxyisocupressic acid (3) and labda-7,13(E)-diene-6beta,15, 17-triol-19-oic acid (4), and Mucor mucedo (ATCC 20094) gave 2alpha-hydroxyisocupressic acid (5) and labda-8(17),14-diene-2alpha, 13-diol-19-oic acid (6).

  13. Acidic aerosol in urban air

    Energy Technology Data Exchange (ETDEWEB)

    Fukuda, M.; Yamaoka, S.; Miyazaki, T.; Oka, M.

    1982-01-01

    The distribution and chemical composition of acidic aerosol in Osaka City were investigated. Samples were collected at five sites in the city from June to September, 1979. Acidic aerosol was determined by the acid-base titration method, sulfate ion by barium chloride turbidimetry, nitrate ion by the xylenol method, and chloride ion by the mercury thiocyanate method. The concentration of acidic aerosol at five sites ranged from 7.7 micrograms per cubic meter to 10.0 micrograms per cubic meter, but mean concentrations in the residential area were slightly higher than those in the industrial area. When acidic aerosol concentrations were compared with concentrations of sulfate, nitrate, and chloride ions, a significant correlation was found between acidic aerosol and sulfate ion. The sum of the ion equivalents of the three types showed good correlation with the acidic aerosol equivalent during the whole period.

  14. Amino Acid Catabolism in Plants.

    Science.gov (United States)

    Hildebrandt, Tatjana M; Nunes Nesi, Adriano; Araújo, Wagner L; Braun, Hans-Peter

    2015-11-02

    Amino acids have various prominent functions in plants. Besides their usage during protein biosynthesis, they also represent building blocks for several other biosynthesis pathways and play pivotal roles during signaling processes as well as in plant stress response. In general, pool sizes of the 20 amino acids differ strongly and change dynamically depending on the developmental and physiological state of the plant cell. Besides amino acid biosynthesis, which has already been investigated in great detail, the catabolism of amino acids is of central importance for adjusting their pool sizes but so far has drawn much less attention. The degradation of amino acids can also contribute substantially to the energy state of plant cells under certain physiological conditions, e.g. carbon starvation. In this review, we discuss the biological role of amino acid catabolism and summarize current knowledge on amino acid degradation pathways and their regulation in the context of plant cell physiology.

  15. Nucleic Acid Vaccines

    Institute of Scientific and Technical Information of China (English)

    LU Shan

    2004-01-01

    @@ Anew method of immunization was discovered in the early 1990s. Several research groups independently demonstrated that direct inoculation of DNA plasmids coding for a specific protein antigen could elicit immune responses against that antigen[1-4].Since in theory the mRNA molecules also have the potential to be translated into the protein antigen, this vaccination approach was officially named by WHO as the nucleic acid vaccination even though the term DNA vaccine has been used more commonly in the literature. This novel approach is considered the fourth generation of vaccines after live attenuated vaccines, killed or inactivated vaccines and recombinant protein based subunit vaccines.

  16. Mycophenolic Acid in Silage

    Science.gov (United States)

    Schneweis, Isabell; Meyer, Karsten; Hörmansdorfer, Stefan; Bauer, Johann

    2000-01-01

    We examined 233 silage samples and found that molds were present in 206 samples with counts between 1 × 103 and 8.9 × 107 (mean, 4.7 × 106) CFU/g. Mycophenolic acid, a metabolite of Penicillium roqueforti, was detected by liquid chromatography-mass spectrometry in 74 (32%) of these samples at levels ranging from 20 to 35,000 (mean, 1,400) μg/kg. This compound has well-known immunosuppressive properties, so feeding with contaminated silage may promote the development of infectious diseases in livestock. PMID:10919834

  17. Kinetics of wet oxidation of formic acid and acetic acid

    Energy Technology Data Exchange (ETDEWEB)

    Shende, R.V.; Mahajani, V.V. [Univ. of Mumbai (India). Dept. of Chemical Technology

    1997-11-01

    Oxidation of lower molecular weight carboxylic acids such as formic, acetic, glyoxalic, and oxalic acids is often the rate-controlling step during wet oxidation (WO) of an aqueous waste stream exhibiting very high chemical oxygen demand (COD). The kinetics of WO of formic acid was studied in the absence and presence of a cupric sulfate as catalyst in the temperature range 150--240 C and oxygen partial pressure range 0.345--1.380 MPa. Wet oxidation of acetic acid was carried out in the presence of cupric sulfate in the temperature range 215--235 C. Homogeneous copper sulfate was found to be a very good catalyst for oxidation of formic acid and acetic acid.

  18. Solid acid catalysis from fundamentals to applications

    CERN Document Server

    Hattori, Hideshi

    2014-01-01

    IntroductionTypes of solid acid catalystsAdvantages of solid acid catalysts Historical overviews of solid acid catalystsFuture outlookSolid Acids CatalysisDefinition of acid and base -Brnsted acid and Lewis acid-Acid sites on surfacesAcid strengthRole of acid sites in catalysisBifunctional catalysisPore size effect on catalysis -shape selectivity-Characterization of Solid Acid Catalysts Indicator methodTemperature programmed desorption (TPD) of ammoniaCalorimetry of adsorption of basic moleculesInfrare

  19. Electrolytic nature of aqueous sulfuric acid. 2. Acidity.

    Science.gov (United States)

    Fraenkel, Dan

    2012-09-27

    In part 1 of this study, I reported that the Debye-Hückel limiting law and the smaller-ion shell (SiS) model of strong electrolyte solutions fit nicely with the experimental mean ionic activity coefficient (γ(±)) of aqueous sulfuric acid as a function of concentration and of temperature when the acid is assumed to be a strong 1-3 electrolyte. Here, I report that the SiS-derived activity coefficient of H(+), γ(H(+)), of the 1-3 acid is comparable to that of aqueous HCl. This agrees with titration curves showing, as well-known, that sulfuric acid in water is parallel in strength to aqueous HCl. The calculated pH is in good accord with the Hammett acidity function, H(0), of aqueous sulfuric acid at low concentration, and differences between the two functions at high concentration are discussed and explained. This pH-H(0) relation is consistent with the literature showing that the H(0) of sulfuric acid (in the 1-9 M range) is similar to those of HCl and the other strong mineral monoprotic acids. The titration of aqueous sulfuric acid with NaOH does not agree with the known second dissociation constant of 0.010 23; rather, the constant is found to be ~0.32 and the acid behaves upon neutralization as a strong diprotic acid practically dissociating in one step. A plausible reaction pathway is offered to explain how the acid may transform, upon base neutralization, from a dissociated H(4)SO(5) (as 3H(+) and HSO(5)(3-)) to a dissociated H(2)SO(4) even though the equilibrium constant of the reaction H(+) + HSO(5)(3-) ↔ SO(4)(2-) + H(2)O, at 25 °C, is 10(-37) (part 1).

  20. Japodic Acid, A Novel Aliphatic Acid from Jatropha podagrica Hook

    OpenAIRE

    Aiyelaagbe, Olapeju O.; Gloer, James B.

    2008-01-01

    A new aliphatic acid named japodic acid (1) with a gem-dimethyl cyclopropane ring has been isolated from the roots of Jatropha podagrica. Its structure was established by 1D and 2D NMR and mass spectrometric data. Two other known compounds, erythrinasinate (2) and fraxidin (3) were also isolated from this plant for the first time. Japodic acid showed mild insect growth inhibition activity against Helicoverpa zea (37% growth reduction at 100 ppm). Fraxidin and erythrinasinate exhibited antibac...

  1. Bile acid interactions with cholangiocytes

    Institute of Scientific and Technical Information of China (English)

    Xuefeng Xia; Heather Francis; Shannon Glaser; Gianfranco Alpini; Gene LeSage

    2006-01-01

    Cholangiocytes are exposed to high concentrations of bile acids at their apical membrane. A selective transporter for bile acids, the Apical Sodium Bile Acid Cotransporter (ASBT) (also referred to as Ibat; gene name Slc10a2)is localized on the cholangiocyte apical membrane. On the basolateral membrane, four transport systems have been identified (t-ASBT, multidrug resistance (MDR)3,an unidentified anion exchanger system and organic solute transporter (Ost) heteromeric transporter, OstαOstβ. Together, these transporters unidirectionally move bile acids from ductal bile to the circulation. Bile acids absorbed by cholangiocytes recycle via the peribiliaryplexus back to hepatocytes for re-secretion into bile.This recycling of bile acids between hepatocytes and cholangiocytes is referred to as the cholehepatic shunt pathway. Recent studies suggest that the cholehepatic shunt pathway may contribute in overall hepatobiliary transport of bile acids and to the adaptation to chronic cholestasis due to extrahepatic obstruction. ASBT is acutely regulated by an adenosine 3', 5'-monophosphate (cAMP)-dependent translocation to the apical membrane and by phosphorylation-dependent ubiquitination and proteasome degradation. ASBT is chronically regulated by changes in gene expression in response to biliary bile acid concentration and inflammatory cytokines.Another potential function of cholangiocyte ASBT is to allow cholangiocytes to sample biliary bile acids in order to activate intracellular signaling pathways. Bile acids trigger changes in intracellular calcium, protein kinase C (PKC), phosphoinositide 3-kinase (PI3K), mitogenactivated protein (MAP) kinase and extracellular signalregulated protein kinase (ERK) intracellular signals.Bile acids significantly alter cholangiocyte secretion,proliferation and survival. Different bile acids have differential effects on cholangiocyte intracellular signals,and in some instances trigger opposing effects on cholangiocyte secretion

  2. Rotational study of the bimolecule acetic acid-fluoroacetic acid

    Science.gov (United States)

    Feng, Gang; Gou, Qian; Evangelisti, Luca; Caminati, Walther

    2017-01-01

    The rotational spectrum of the acetic acid-fluoroacetic acid bimolecule was measured by using a pulsed jet Fourier transform microwave spectrometer. One conformer, in which fluoroacetic acid is in trans form, has been observed. The rotational transitions are split into two component lines, due to the internal rotation of the methyl group of acetic acid. From these splittings, the corresponding V3 barrier has been determined. The dissociation energy of this complex has been estimated to 66 kJ/mol. An increase of the distance between the two monomers upon the OH → OD substitution (Ubbelohde effect) has been observed.

  3. Esterification by the Plasma Acidic Water: Novel Application of Plasma Acid

    Science.gov (United States)

    Gu, Ling

    2014-03-01

    This work explores the possibility of plasma acid as acid catalyst in organic reactions. Plasma acidic water was prepared by dielectric barrier discharge and used to catalyze esterification of n-heptanioc acid with ethanol. It is found that the plasma acidic water has a stable and better performance than sulfuric acid, meaning that it is an excellent acid catalyst. The plasma acidic water would be a promising alternative for classic mineral acid as a more environment friendly acid.

  4. Molecular Simulation of Naphthenic Acid Removal on Acidic Catalyst Ⅱ. Experimental results of catalytic decarboxylation over acidic catalysts

    Institute of Scientific and Technical Information of China (English)

    Fu Xiaoqin; Tian Songbai; Hou Shuandi; Longjun; Wang Xieqing

    2008-01-01

    The energy barriers of thermal decarboxylation reactions of petroleum acids and catalytic decarboxylation reactions of Br(o)nsted acid and Lewis acid were analyzed using molecular simulation technology.Compared with thermal decarboxylation reactions of petroleum acids, the decarboxylation reactions by acid catalysts were easier to occur. The decarboxylaton effect by Lewis acid was better than Br(o)nsted acid. The mechanisms of catalytic decarboxylation over acid catalyst were also verified by experiments on a fixed bed and a fluidized bed, the experimental results showed that the rate of acid removal could reach up to 97% over the acidic catalyst at a temperature above 400℃.

  5. Synthesis of aminoaldonic acids

    DEFF Research Database (Denmark)

    Jørgensen, Christel Thea

    With the aim of synthesising aminoaldonic acids, two 2-acetamido-2-deoxyaldonolactones with D-galacto (6) and D-arabino (11) configuration were prepared from acetylated sugar formazans in analogy with a known procedure. Empolying the same procedure to acetylated sugar phenylhydrazones gave mixtures...... and 82, respectively. The aminolactone 84 was converted into the corresponding amino sugar 89.With the aim of synthesising substrates for the Pictet-Spengler reaction three 4-aldehydo acetamidodideoxytetronolactones 92, 97 and 103 were prepared by periodate cleavage of the corresponding hexonolactones......,4-lactone, respectively. A 2,3-aziridino-2,3-dideoxypentonamide 70 was also prepared from D-glucono-1,5-lactone. The lactones were converted into methyl 3,4-O-isopropylidene-2-O-sulfonyl esters 42, 50, 62 and 68, which upon treatment with concentrated aqueous ammonia yielded the aziridino compounds...

  6. Acid mine drainage

    Science.gov (United States)

    Bigham, Jerry M.; Cravotta, Charles A.

    2016-01-01

    Acid mine drainage (AMD) consists of metal-laden solutions produced by the oxidative dissolution of iron sulfide minerals exposed to air, moisture, and acidophilic microbes during the mining of coal and metal deposits. The pH of AMD is usually in the range of 2–6, but mine-impacted waters at circumneutral pH (5–8) are also common. Mine drainage usually contains elevated concentrations of sulfate, iron, aluminum, and other potentially toxic metals leached from rock that hydrolyze and coprecipitate to form rust-colored encrustations or sediments. When AMD is discharged into surface waters or groundwaters, degradation of water quality, injury to aquatic life, and corrosion or encrustation of engineered structures can occur for substantial distances. Prevention and remediation strategies should consider the biogeochemical complexity of the system, the longevity of AMD pollution, the predictive power of geochemical modeling, and the full range of available field technologies for problem mitigation.

  7. Enzymatic tRNA acylation by acid and alpha-hydroxy acid analogues of amino acids.

    Science.gov (United States)

    Owczarek, Alina; Safro, Mark; Wolfson, Alexey D

    2008-01-08

    Incorporation of unnatural amino acids with unique chemical functionalities has proven to be a valuable tool for expansion of the functional repertoire and properties of proteins as well as for structure-function analysis. Incorporation of alpha-hydroxy acids (primary amino group is substituted with hydroxyl) leads to the synthesis of proteins with peptide bonds being substituted by ester bonds. Practical application of this modification is limited by the necessity to prepare corresponding acylated tRNA by chemical synthesis. We investigated the possibility of enzymatic incorporation of alpha-hydroxy acid and acid analogues (lacking amino group) of amino acids into tRNA using aminoacyl-tRNA synthetases (aaRSs). We studied direct acylation of tRNAs by alpha-hydroxy acid and acid analogues of amino acids and corresponding chemically synthesized analogues of aminoacyl-adenylates. Using adenylate analogues we were able to enzymatically acylate tRNA with amino acid analogues which were otherwise completely inactive in direct aminoacylation reaction, thus bypassing the natural mechanisms ensuring the selectivity of tRNA aminoacylation. Our results are the first demonstration that the use of synthetic aminoacyl-adenylates as substrates in tRNA aminoacylation reaction may provide a way for incorporation of unnatural amino acids into tRNA, and consequently into proteins.

  8. Ghrelin and gastric acid secretion.

    Science.gov (United States)

    Yakabi, Koji; Kawashima, Junichi; Kato, Shingo

    2008-11-07

    Ghrelin, a novel growth hormone-releasing peptide, was originally isolated from rat and human stomach. Ghrelin has been known to increase the secretion of growth hormone (GH), food intake, and body weight gain when administered peripherally or centrally. Ghrelin is also known to stimulate the gastric motility and the secretion of gastric acid. In the previous studies, the action of ghrelin on acid secretion was shown to be as strong as that of histamine and gastrin in in-vivo experiment. In the studies, the mechanism for the action of ghrelin was also investigated. It was shown that vagotomy completely inhibited the action of ghrelin on the secretion of gastric acid suggesting that vagal nerve is involved in the mechanism for the action of ghrelin on acid secretion. As famotidine did not inhibit ghrelin-induced acid secretion in the study by Masuda et al, they concluded that histamine was not involved in the action of ghrelin on acid secretion. However, we have shown that famotidine completely inhibited ghrelin-induced acid secretion and histidine decarboxylase (HDC) mRNA was increased in gastric mucosa by ghrelin injection which is inhibited by vagotomy Our results indicate that histamine is involved in the action of ghrelin on acid secretion. Furthermore synergistic action of gastrin and ghrelin on gastric acid secretion was shown. Although gastrin has important roles in postprandial secretion of gastric acid, ghrelin may be related to acid secretion during fasting period or at night. However, further studies are needed to elucidate the physiological role of ghrelin in acid secretion.

  9. Racemization of Meteoritic Amino Acids

    Science.gov (United States)

    Cohen, Barbara A.; Chyba, Christopher F.

    2000-05-01

    Meteorites may have contributed amino acids to the prebiotic Earth, affecting the global ratio of right-handed to left-handed (D/L) molecules. We calculate D/L ratios for seven biological, α-hydrogen, protein amino acids over a variety of plausible parent body thermal histories, based on meteorite evidence and asteroid modeling. We show that amino acids in meteorites do not necessarily undergo complete racemization by the time they are recovered on Earth. If the mechanism of amino acid formation imposes some enantiomeric preference on the amino acids, a chiral signature can be retained through the entire history of the meteorite. Original enantiomeric excesses in meteorites such as Murchison, which have undergone apparently short and cool alteration scenarios, should have persisted to the present time. Of the seven amino acids for which relevant data are available, we expect glutamic acid, isoleucine, and valine, respectively, to be the most likely to retain an initial enantiomeric excess, and phenylalanine, aspartic acid, and alanine the least. Were the D/L ratio initially identical in each amino acid, final D/L ratios could be used to constrain the initial ratio and the thermal history experienced by the whole suite.

  10. [Hydrofluoric acid poisoning: case report].

    Science.gov (United States)

    Cortina, Tatiana Judith; Ferrero, Hilario Andrés

    2013-01-01

    Hydrofluoric acid is a highly dangerous substance with industrial and domestically appliances. Clinical manifestations of poisoning depend on exposure mechanism, acid concentration and exposed tissue penetrability. Gastrointestinal tract symptoms do not correlate with injury severity. Patients with history of hydrofluoric acid ingestion should undergo an endoscopy of the upper gastrointestinal tract. Intoxication requires immediate intervention because systemic toxicity can take place. We present a 5 year old girl who accidentally swallowed 5 ml of 20% hydrofluoric acid. We performed gastrointestinal tract endoscopy post ingestion, which revealed erythematous esophagus and stomach with erosive lesions. Two months later, same study was performed and revealed esophagus and stomach normal mucous membrane.

  11. Preparation and characterization Al3+-bentonite Turen Malang for esterification fatty acid (palmitic acid, oleic acid and linoleic acid)

    Science.gov (United States)

    Abdulloh, Abdulloh; Aminah, Nanik Siti; Triyono, Mudasir, Trisunaryanti, Wega

    2016-03-01

    Catalyst preparation and characterization of Al3+-bentonite for esterification of palmitic acid, oleic acid and linoleic acid has been done. Al3+-bentonite catalyst was prepared from natural bentonite of Turen Malang through cation exchange reaction using AlCl3 solution. The catalysts obtained were characterized by XRD, XRF, pyridine-FTIR and surface area analyser using the BET method. Catalyst activity test of Al3+-bentonite for esterification reaction was done at 65°C using molar ratio of metanol-fatty acid of 30:1 and 0.25 g of Al3+-bentonite catalyst for the period of ½, 1, 2, 3, 4 and 5 hours. Based on the characterization results, the Al3+-bentonite Turen Malang catalyst has a d-spacing of 15.63 Ǻ, acid sites of Brönsted and Lewis respectively of 230.79 µmol/g and 99.39 µmol/g, surface area of 507.3 m2/g and the average of radius pore of 20.09 Å. GC-MS analysis results of the oil phase after esterification reaction showed the formation of biodiesel (FAME: Fatty acid methyl ester), namely methyl palmitate, methyl oleate and methyl linoleate. The number of conversions resulted in esterification reaction using Al3+-bentonite Turen Malang catalyst was 74.61%, 37.75%, and 20, 93% for the esterification of palmitic acid, oleic acid and linoleic acid respectively.

  12. Antibiofilm Properties of Acetic Acid

    DEFF Research Database (Denmark)

    Bjarnsholt, Thomas; Alhede, Morten; Jensen, Peter Østrup;

    2014-01-01

    of the infected implant, tissue, or organ and thereby the biofilm. Acetic acid is known for its antimicrobial effect on bacteria in general, but has never been thoroughly tested for its efficacy against bacterial biofilms. In this article, we describe complete eradication of both Gram-positive and Gram......-negative biofilms using acetic acid both as a liquid and as a dry salt. In addition, we present our clinical experience of acetic acid treatment of chronic wounds. In conclusion, we here present the first comprehensive in vitro and in vivo testing of acetic acid against bacterial biofilms....

  13. 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....

  14. Peptide Nucleic Acids Having Amino Acid Side Chains

    DEFF Research Database (Denmark)

    1998-01-01

    A novel class of compounds, known as peptide nucleic acids, bind complementary DNA and RNA strands more strongly than the corresponding DNA or RNA strands, and exhibit increased sequence specificity and solubility. The peptide nucleic acids comprise ligands selected from a group consisting...

  15. Fatty Acid Desaturases, Polyunsaturated Fatty Acid Regulation, and Biotechnological Advances

    Directory of Open Access Journals (Sweden)

    Je Min Lee

    2016-01-01

    Full Text Available Polyunsaturated fatty acids (PUFAs are considered to be critical nutrients to regulate human health and development, and numerous fatty acid desaturases play key roles in synthesizing PUFAs. Given the lack of delta-12 and -15 desaturases and the low levels of conversion to PUFAs, humans must consume some omega-3 and omega-6 fatty acids in their diet. Many studies on fatty acid desaturases as well as PUFAs have shown that fatty acid desaturase genes are closely related to different human physiological conditions. Since the first front-end desaturases from cyanobacteria were cloned, numerous desaturase genes have been identified and animals and plants have been genetically engineered to produce PUFAs such as eicosapentaenoic acid and docosahexaenoic acid. Recently, a biotechnological approach has been used to develop clinical treatments for human physiological conditions, including cancers and neurogenetic disorders. Thus, understanding the functions and regulation of PUFAs associated with human health and development by using biotechnology may facilitate the engineering of more advanced PUFA production and provide new insights into the complexity of fatty acid metabolism.

  16. Fatty Acid Desaturases, Polyunsaturated Fatty Acid Regulation, and Biotechnological Advances.

    Science.gov (United States)

    Lee, Je Min; Lee, Hyungjae; Kang, SeokBeom; Park, Woo Jung

    2016-01-04

    Polyunsaturated fatty acids (PUFAs) are considered to be critical nutrients to regulate human health and development, and numerous fatty acid desaturases play key roles in synthesizing PUFAs. Given the lack of delta-12 and -15 desaturases and the low levels of conversion to PUFAs, humans must consume some omega-3 and omega-6 fatty acids in their diet. Many studies on fatty acid desaturases as well as PUFAs have shown that fatty acid desaturase genes are closely related to different human physiological conditions. Since the first front-end desaturases from cyanobacteria were cloned, numerous desaturase genes have been identified and animals and plants have been genetically engineered to produce PUFAs such as eicosapentaenoic acid and docosahexaenoic acid. Recently, a biotechnological approach has been used to develop clinical treatments for human physiological conditions, including cancers and neurogenetic disorders. Thus, understanding the functions and regulation of PUFAs associated with human health and development by using biotechnology may facilitate the engineering of more advanced PUFA production and provide new insights into the complexity of fatty acid metabolism.

  17. Carbonic Acid Pretreatment of Biomass

    Energy Technology Data Exchange (ETDEWEB)

    G. Peter van Walsum; Kemantha Jayawardhana; Damon Yourchisin; Robert McWilliams; Vanessa Castleberry

    2003-05-31

    This project sought to address six objectives, outlined below. The objectives were met through the completion of ten tasks. 1) Solidify the theoretical understanding of the binary CO2/H2O system at reaction temperatures and pressures. The thermodynamics of pH prediction have been improved to include a more rigorous treatment of non-ideal gas phases. However it was found that experimental attempts to confirm theoretical pH predictions were still off by a factor of about 1.8 pH units. Arrhenius experiments were carried out and the activation energy for carbonic acid appears to be substantially similar to sulfuric acid. Titration experiments have not yet confirmed or quantified the buffering or acid suppression effects of carbonic acid on biomass. 2) Modify the carbonic acid pretreatment severity function to include the effect of endogenous acid formation and carbonate buffering, if necessary. It was found that the existing severity functions serve adequately to account for endogenous acid production and carbonate effects. 3) Quantify the production of soluble carbohydrates at different reaction conditions and severity. Results show that carbonic acid has little effect on increasing soluble carbohydrate concentrations for pretreated aspen wood, compared to pretreatment with water alone. This appears to be connected to the release of endogenous acids by the substrate. A less acidic substrate such as corn stover would derive benefit from the use of carbonic acid. 4) Quantify the production of microbial inhibitors at selected reaction conditions and severity. It was found that the release of inhibitors was correlated to reaction severity and that carbonic acid did not appear to increase or decrease inhibition compared to pretreatment with water alone. 5) Assess the reactivity to enzymatic hydrolysis of material pretreated at selected reaction conditions and severity. Enzymatic hydrolysis rates increased with severity, but no advantage was detected for the use of carbonic

  18. Carbonic Acid Retreatment of Biomass

    Energy Technology Data Exchange (ETDEWEB)

    Baylor university

    2003-06-01

    This project sought to address six objectives, outlined below. The objectives were met through the completion of ten tasks. (1) Solidify the theoretical understanding of the binary CO{sub 2}/H{sub 2}O system at reaction temperatures and pressures. The thermodynamics of pH prediction have been improved to include a more rigorous treatment of non-ideal gas phases. However it was found that experimental attempts to confirm theoretical pH predictions were still off by a factor of about 1.8 pH units. Arrhenius experiments were carried out and the activation energy for carbonic acid appears to be substantially similar to sulfuric acid. Titration experiments have not yet confirmed or quantified the buffering or acid suppression effects of carbonic acid on biomass. (2) Modify the carbonic acid pretreatment severity function to include the effect of endogenous acid formation and carbonate buffering, if necessary. It was found that the existing severity functions serve adequately to account for endogenous acid production and carbonate effects. (3) Quantify the production of soluble carbohydrates at different reaction conditions and severity. Results show that carbonic acid has little effect on increasing soluble carbohydrate concentrations for pretreated aspen wood, compared to pretreatment with water alone. This appears to be connected to the release of endogenous acids by the substrate. A less acidic substrate such as corn stover would derive benefit from the use of carbonic acid. (4) Quantify the production of microbial inhibitors at selected reaction conditions and severity. It was found that the release of inhibitors was correlated to reaction severity and that carbonic acid did not appear to increase or decrease inhibition compared to pretreatment with water alone. (5) Assess the reactivity to enzymatic hydrolysis of material pretreated at selected reaction conditions and severity. Enzymatic hydrolysis rates increased with severity, but no advantage was detected for

  19. Ghrelin and gastric acid secretion

    Institute of Scientific and Technical Information of China (English)

    Koji Yakabi; Junichi Kawashima; Shingo Kato

    2008-01-01

    Ghrelin, a novel growth hormone-releasing peptide, was originally isolated from rat and human stomach. Ghrelin has been known to increase the secretion of growth hormone (GH), food intake, and body weight gain when administered peripherally or centrally. Ghrelin is also known to stimulate the gastric motility and the secretion of gastric acid. In the previous studies, the action of ghrelin on acid secretion was shown to be as strong as that of histamine and gastrin in-vivo experiment. In the studies, the mechanism for the action of ghrelin was also investigated. It was shown that vagotomy completely inhibited the action of ghrelin on the secretion of gastric acid suggesting that vagal nerve is involved in the mechanism for the action of ghrelin on acid secretion. As famotidine did not inhibit ghrelin-in-duced acid secretion in the study by Masuda et al, they concluded that histamine was not involved in the action of ghrelin on acid secretion. However, we have shown that famotidine completely inhibited ghrelin-induced acid secretion and histidine decarboxylase (HDC) mRNA was increased in gastric mucosa by ghrelin injection which is inhibited by vagotomy Our results indicate that histamine is involved in the action of ghrelin on acid secretion. Furthermore synergistic action of gastrin and ghrelin on gastric add secretion was shown. Although gastrin has important roles in postprandial secretion of gastric acid, ghrelin may be related to acid secretion during fasting period or at night. However, further studies are needed to elucidate the physiological role of ghrelin in acid secretion.

  20. Amino acids in Arctic aerosols

    Directory of Open Access Journals (Sweden)

    E. Scalabrin

    2012-07-01

    Full Text Available Amino acids are significant components of atmospheric aerosols, affecting organic nitrogen input to marine ecosystems, atmospheric radiation balance, and the global water cycle. The wide range of amino acid reactivities suggest that amino acids may serve as markers of atmospheric transport and deposition of particles. Despite this potential, few measurements have been conducted in remote areas to assess amino acid concentrations and potential sources. Polar regions offer a unique opportunity to investigate atmospheric processes and to conduct source apportionment studies of such compounds. In order to better understand the importance of amino acid compounds in the global atmosphere, we determined free amino acids (FAAs in seventeen size-segregated aerosol samples collected in a polar station in the Svalbard Islands from 19 April until 14 September 2010. We used an HPLC coupled with a tandem mass spectrometer (ESI-MS/MS to analyze 20 amino acids to quantify compounds at fmol m−3 levels. Mean total FAA concentration was 1070 fmol m−3 where serine and glycine were the most abundant compounds in almost all samples and accounted for 45–60% of the total amino acid relative abundance. The other eighteen compounds had average concentrations between 0.3 and 98 fmol m−3. The higher amino acid concentrations were present in the ultrafine aerosol fraction (<0.49 μm and accounted for the majority of the total amino acid content. Local marine sources dominate the boreal summer amino acid concentrations, with the exception of the regional input from Icelandic volcanics.

  1. Production of succinic Acid from citric Acid and related acids by lactobacillus strains.

    Science.gov (United States)

    Kaneuchi, C; Seki, M; Komagata, K

    1988-12-01

    A number of Lactobacillus strains produced succinic acid in de Man-Rogosa-Sharpe broth to various extents. Among 86 fresh isolates from fermented cane molasses in Thailand, 30 strains (35%) produced succinic acid; namely, 23 of 39 Lactobacillus reuteri strains, 6 of 18 L. cellobiosus strains, and 1 of 6 unidentified strains. All of 10 L. casei subsp. casei strains, 5 L. casei subsp. rhamnosus strains, 6 L. mali strains, and 2 L. buchneri strains did not produce succinic acid. Among 58 known strains including 48 type strains of different Lactobacillus species, the strains of L. acidophilus, L. crispatus, L. jensenii, and L. parvus produced succinic acid to the same extent as the most active fresh isolates, and those of L. alimentarius, L. collinoides, L. farciminis, L. fructivorans (1 of 2 strains tested), L. malefermentans, and L. reuteri were also positive, to lesser extents. Diammonium citrate in de Man-Rogosa-Sharpe broth was determined as a precursor of the succinic acid produced. Production rates were about 70% on a molar basis with two fresh strains tested. Succinic acid was also produced from fumaric and malic acids but not from dl-isocitric, alpha-ketoglutaric, and pyruvic acids. The present study is considered to provide the first evidence on the production of succinic acid, an important flavoring substance in dairy products and fermented beverages, from citrate by lactobacilli.

  2. Kwas acetylosalicylowy i jego zastosowanie w profilaktyce chorób u kobiet po menopauzie

    Directory of Open Access Journals (Sweden)

    Ireneusz Połać

    2011-02-01

    Full Text Available Acetylsalicylic acid (ASA is a simple chemical compound belonging to a group of nonsteroidal antiinflammatorydrugs (NSAIDs. The mechanism of acetylsalicylic acid is based on the inhibition of cyclooxygenase(COX. That enzyme is responsible for the biosynthesis of cyclic prostanoids, i.e. prostaglandins (D2, E2, F2, I2,thromboxane A2 (TXA2 and prostacyclin. For this reason ASA is one of the most popular anti-inflammatorydrugs present on the pharmaceutical market. Due to its ability to inhibit the synthesis of TXA2 (moleculescapable of platelet activation ASA is effective in the prevention of cardiovascular diseases such as ischemicheart disease. Clinical trials confirm the efficacy of aspirin in the prevention of cardiovascular diseases inpostmenopausal women. In some cases ASA is unable to inhibit platelet activation. This phenomenon iscalled aspirin resistance. Acetylsalicylic acid can also inhibit aromatase activity, therefore it may be used inthe prevention of breast cancer. Many clinical trials confirm that acetylsalicylic acid reduces the risk of breastcancer in postmenopausal women. Use of ASA may also increase bone mineral density (BMD. This articledescribes the mechanism of action and pharmacokinetics of the acetylsalicylic acid as well as clinical trialsconducted on postmenopausal women.

  3. Bile acids for viral hepatitis

    DEFF Research Database (Denmark)

    Chen, Weikeng; Liu, J; Gluud, C

    2003-01-01

    The viral hepatitides are common causes of liver diseases globally. Trials have assessed bile acids for patients with viral hepatitis, but no consensus was reached regarding their usefulness.......The viral hepatitides are common causes of liver diseases globally. Trials have assessed bile acids for patients with viral hepatitis, but no consensus was reached regarding their usefulness....

  4. Protein and amino acid nutrition

    Science.gov (United States)

    Dairy cow protein and amino acid nutrition have a significant role in sustainable dairying. Protein, amino acids, and nitrogen are inextricably linked through effects in the rumen, metabolism of the cow, and environmental nutrient management. Feeding systems have been making progress toward emphasiz...

  5. Phosphorus derivatives of salicylic acid

    Science.gov (United States)

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

    1992-10-01

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

  6. Pantothenic acid (Vitamin B5)

    Science.gov (United States)

    ... vitamin B5 (pantothenic acid), vitamin B6 (pyridoxine), vitamin B12 (cyanocobalamin), and folic acid. However, some products do ... Pantothenas, Calcium D-Pantothenate, Calcium Pantothenate, Complexe de Vitamines B, D-Calcium Pantothenate, D-Panthenol, D-Panthénol, ...

  7. Acid Rain: The Scientific Challenge.

    Science.gov (United States)

    Godfrey, Paul J.

    1991-01-01

    Documents the workings and findings of the Massachusetts Acid Rain Monitoring Project, which has pooled the volunteer efforts of more than 1,000 amateur and professional scientists since 1983. Reports on the origins of air pollution, the prediction of acid rain, and its effects on both water life and land resources. (JJK)

  8. Acid Rain: What's the Forecast?

    Science.gov (United States)

    Bybee, Rodger

    1984-01-01

    Discusses various types of acid rain, considered to be a century-old problem. Topics include: wet and dry deposition, effects on a variety of environments, ecosystems subject to detrimental effects, and possible solutions to the problem. A list of recommended resources on acid rain is provided. (BC)

  9. Kinetics and Mechanism of Oxidation of Phenyl Acetic Acid and Dl-Mandelic Acid by Permanganate in Acid Medium

    Directory of Open Access Journals (Sweden)

    B.Syama Sundar

    2014-06-01

    Full Text Available Kinetics of oxidation of phenyl acetic acid and DL- Mandelic acid by potassium permanganate in aqueous acetic acid and perchloric acid mixture reveals that the kinetic orders are first order in oxidant, first order in H+ and zero order in substrate for phenyl acetic acid. DL-Mandelic acid exhibits first order in oxidant and zero order in substrate. The results are rationalised by a mechanism involving intermediate formation of mandelic acid in case of Phenyl acetic acid and ester formation with Mn (VII in case of DL-Mandelic acid. The following order of reactivity is observed: DL-Mandelic acid > Phenyl acetic acid. The high reactivity of DL-Mandelic acid over phenyl acetic acid may be due to different mechanisms operating with the two substrates and benzaldehyde is the final product in both the cases.

  10. N-(3-Nitrophenylmaleamic acid

    Directory of Open Access Journals (Sweden)

    B. Thimme Gowda

    2010-07-01

    Full Text Available In the title compound, C10H8N2O5, the molecule is slightly distorted from planarity. The molecular structure is stabilized by two intramolecular hydrogen bonds. The first is a short O—H...O hydrogen bond (H...O distance = 1.57 Å within the maleamic acid unit and the second is a C—H...O hydrogen bond (H...O distance = 2.24 Å which connects the amide group with the benzene ring. The nitro group is twisted by 6.2 (2° out of the plane of the benzene ring. The crystal structure manifests a variety of hydrogen bonding. The packing is dominated by a strong intermolecular N—H...O interaction which links the molecules into chains running along the b axis. The chains within a plane are further assembled by three additional types of intermolecular C—H...O hydrogen bonds to form a sheet parallel to the (overline{1}01 plane.

  11. Molten fatty acid based microemulsions.

    Science.gov (United States)

    Noirjean, Cecile; Testard, Fabienne; Dejugnat, Christophe; Jestin, Jacques; Carriere, David

    2016-06-21

    We show that ternary mixtures of water (polar phase), myristic acid (MA, apolar phase) and cetyltrimethylammonium bromide (CTAB, cationic surfactant) studied above the melting point of myristic acid allow the preparation of microemulsions without adding a salt or a co-surfactant. The combination of SANS, SAXS/WAXS, DSC, and phase diagram determination allows a complete characterization of the structures and interactions between components in the molten fatty acid based microemulsions. For the different structures characterized (microemulsion, lamellar or hexagonal phases), a similar thermal behaviour is observed for all ternary MA/CTAB/water monophasic samples and for binary MA/CTAB mixtures without water: crystalline myristic acid melts at 52 °C, and a thermal transition at 70 °C is assigned to the breaking of hydrogen bounds inside the mixed myristic acid/CTAB complex (being the surfactant film in the ternary system). Water determines the film curvature, hence the structures observed at high temperature, but does not influence the thermal behaviour of the ternary system. Myristic acid is partitioned in two "species" that behave independently: pure myristic acid and myristic acid associated with CTAB to form an equimolar complex that plays the role of the surfactant film. We therefore show that myristic acid plays the role of a solvent (oil) and a co-surfactant allowing the fine tuning of the structure of oil and water mixtures. This solvosurfactant behaviour of long chain fatty acid opens the way for new formulations with a complex structure without the addition of any extra compound.

  12. Pentadecanoic and Heptadecanoic Acids: Multifaceted Odd-Chain Fatty Acids.

    Science.gov (United States)

    Pfeuffer, Maria; Jaudszus, Anke

    2016-07-01

    The odd-chain fatty acids (OCFAs) pentadecanoic acid (15:0) and heptadecanoic acid (17:0), which account for only a small proportion of total saturated fatty acids in milk fat and ruminant meat, are accepted biomarkers of dairy fat intake. However, they can also be synthesized endogenously, for example, from gut-derived propionic acid (3:0). A number of studies have shown an inverse association between OCFA concentrations in human plasma phospholipids or RBCs and risk of type 2 diabetes and cardiovascular disease. We propose a possible involvement in metabolic regulation from the assumption that there is a link between 15:0 and 17:0 and the metabolism of other short-chain, medium-chain, and longer-chain OCFAs. The OCFAs 15:0 and 17:0 can be elongated to very-long-chain FAs (VLCFAs) such as tricosanoic acid (23:0) and pentacosanoic acid (25:0) in glycosphingolipids, particularly found in brain tissue, or can be derived from these VLCFAs. Their chains can be shortened, yielding propionyl-coenzyme A (CoA). Propionyl-CoA, by succinyl-CoA, can replenish the citric acid cycle (CAC) with anaplerotic intermediates and, thus, improve mitochondrial energy metabolism. Mitochondrial function is compromised in a number of disorders and may be impaired with increasing age. Optimizing anaplerotic intermediate availability for the CAC may help to cope with demands in times of increased metabolic stress and with aging. OCFAs may serve as substrates for synthesis of both odd-numbered VLCFAs and propionyl-CoA or store away excess propionic acid.

  13. Fatty acid composition of selected prosthecate bacteria.

    Science.gov (United States)

    Carter, R N; Schmidt, J M

    1976-10-11

    The cellular fatty acid composition of 14 strains of Caulobacter speices and types, two species of Prosthecomicrobium, and two species of Asticcacaulis was determined by gas-liquid chromatography. In most of these bacteria, the major fatty acids were octadecenoic acid (C18:1), hexadecenoic acid (C16:1) and hexadecanoic acid (C16:0). Some cyclopropane and branched chain fatty acids were detected in addition to the straight chained acids. Hydroxytetradecanoic acid was an important component of P.enhydrum but significant amounts of hydroxy acids were not detected in other prosthecate bacteria examined.

  14. The Property and Application of Arachidonic Acid

    Institute of Scientific and Technical Information of China (English)

    王相勤; 姚建铭; 袁成凌; 王纪; 余增亮

    2002-01-01

    Arachidonic acid (AA) is one of the most important PUFAs (polyunsaturated fatty acids) in human body. A high-yield arachidonic acid-producing strain (mortierella alpina) was selected by ion implantation (the relative content of arachidonic acid is 70.2% among all fatty acids). This paper mainly introduced the structure, distribution, source, physiologic healthcare function and application of AA.

  15. Phytic acid in green leaves.

    Science.gov (United States)

    Hadi Alkarawi, H; Zotz, G

    2014-07-01

    Phytic acid or phytate, the free-acid form of myo-inositolhexakiphosphate, is abundant in many seeds and fruits, where it represents the major storage form of phosphorus. Although also known from other plant tissues, available reports on the occurrence of phytic acid, e.g. in leaves, have never been compiled, nor have they been critically reviewed. We found 45 published studies with information on phytic acid content in leaves. Phytic acid was almost always detected when studies specifically tried to detect it, and accounted for up to 98% of total P. However, we argue that such extreme values, which rival findings from storage organs, are dubious and probably result from measurement errors. Excluding these high values from further quantitative analysis, foliar phytic acid-P averaged 2.3 mg·g(-1) , and represented, on average, 7.6% of total P. Remarkably, the ratio of phytic acid-P to total P did not increase with total P, we even detected a negative correlation of the two variables within one species, Manihot esculenta. This enigmatic finding warrants further attention.

  16. Terahertz spectrum of gallic acid

    Science.gov (United States)

    Wu, Meng; Zhao, Guozhong; Wang, Haiyan; Liang, Chengshen

    2009-11-01

    Gallic acid is natural polyphenol compound found in many green plants. More and more experiments have demonstrated that the gallic acid has comprehensive applications. In the field of medicine, the gallic acid plays an important role in antianaphylaxis, antineoplastic, antimycotic, anti-inflammatory, antivirotic, antiasthmatic and inhibiting the degradation of insulin. It also has a lot of applications in chemical industry, food industry and light industry. So it is important to study the terahertz time-domain spectroscopy of gallic acid. Terahertz time-domain spectroscopy (THz-TDS) is a new coherent spectral technology based on the femtosecond laser. In this work, the spectral characteristics of gallic acid in the range of 0.4 THz to 2.6 THz have been measured by THz-TDS. We obtained its absorption and refraction spectra at room temperature. The vibration absorption spectrum of the single molecule between 0.4 THz and 2.6 THz is simulated based on the Density Functional Theory (DFT). It is found that the gallic acid has the spectral response to THz wave in this frequency range. The results show the abnormal dispersion at 1.51 THz and 2.05 THz. These results can be used in the qualitative analysis of gallic acid and the medicine and food inspection.

  17. Determination of polyfluoroalkyl phosphoric acid diesters, perfluoroalkyl phosphonic acids, perfluoroalkyl phosphinic acids, perfluoroalkyl carboxylic acids, and perfluoroalkane sulfonic acids in lake trout from the Great Lakes region.

    Science.gov (United States)

    Guo, Rui; Reiner, Eric J; Bhavsar, Satyendra P; Helm, Paul A; Mabury, Scott A; Braekevelt, Eric; Tittlemier, Sheryl A

    2012-11-01

    A comprehensive method to extract perfluoroalkyl carboxylic acids, perfluoroalkane sulfonic acids, perfluoroalkyl phosphonic acids, perfluoroalkyl phosphinic acids, and polyfluoroalkyl phosphoric acid diesters simultaneously from fish samples has been developed. The recoveries of target compounds ranged from 78 % to 121 %. The new method was used to analyze lake trout (Salvelinus namaycush) from the Great Lakes region. The results showed that the total perfluoroalkane sulfonate concentrations ranged from 0.1 to 145 ng/g (wet weight) with perfluorooctane sulfonate (PFOS) as the dominant contaminant. Concentrations in fish between lakes were in the order of Lakes Ontario ≈ Erie > Huron > Superior ≈ Nipigon. The total perfluoroalkyl carboxylic acid concentrations ranged from 0.2 to 18.2 ng/g wet weight. The aggregate mean perfluorooctanoic acid (PFOA) concentration in fish across all lakes was 0.045 ± 0.023 ng/g. Mean concentrations of PFOA were not significantly different (p > 0.1) among the five lakes. Perfluoroalkyl phosphinic acids were detected in lake trout from Lake Ontario, Lake Erie, and Lake Huron with concentration ranging from non-detect (ND) to 0.032 ng/g. Polyfluoroalkyl phosphoric acid diesters were detected only in lake trout from Lake Huron, at levels similar to perfluorooctanoic acid.

  18. Pyroligneous acid-the smoky acidic liquid from plant biomass.

    Science.gov (United States)

    Mathew, Sindhu; Zakaria, Zainul Akmar

    2015-01-01

    Pyroligneous acid (PA) is a complex highly oxygenated aqueous liquid fraction obtained by the condensation of pyrolysis vapors, which result from the thermochemical breakdown or pyrolysis of plant biomass components such as cellulose, hemicellulose, and lignin. PA produced by the slow pyrolysis of plant biomass is a yellowish brown or dark brown liquid with acidic pH and usually comprises a complex mixture of guaiacols, catechols, syringols, phenols, vanillins, furans, pyrans, carboxaldehydes, hydroxyketones, sugars, alkyl aryl ethers, nitrogenated derivatives, alcohols, acetic acid, and other carboxylic acids. The phenolic components, namely guaiacol, alkyl guaiacols, syringol, and alkyl syringols, contribute to the smoky odor of PA. PA finds application in diverse areas, as antioxidant, antimicrobial, antiinflammatory, plant growth stimulator, coagulant for natural rubber, and termiticidal and pesticidal agent; is a source for valuable chemicals; and imparts a smoky flavor for food.

  19. ELECTRODIALYTIC PRODUCTION OF HYPOPHOSPHOROUS ACID

    Institute of Scientific and Technical Information of China (English)

    CHENG Jianzhong; ZHANG Yingzhe; ZHANG Baogui; ZHANG Zhengpu

    2001-01-01

    Disclosed is a method of preparing hypophosphorous acid comprising contacting an insoluble anode with an aqueous solution of hypophosphite anions and applying a direct current through the insoluble anode to a cathode in electrical contact with the aqueous solution to generate H+ ions in the aqueous solution thereby forming a hypophosphorous acid solution. The process is simple,low cost and high efficient, which can be tied into an existing process for producing sodium hypophosphite wherein the product of sodium hypophosphite process is used as a starting material in the hypophosphorous acid process.

  20. Amino Acids from a Comet

    Science.gov (United States)

    Cook, Jamie Elisla

    2009-01-01

    NASA's Stardust spacecraft returned samples from comet 81P/Wild 2 to Earth in January 2006. Examinations of the organic compounds in cometary samples can reveal information about the prebiotic organic inventory present on the early Earth and within the early Solar System, which may have contributed to the origin of life. Preliminary studies of Stardust material revealed the presence of a suite of organic compounds including several amines and amino acids, but the origin of these compounds (cometary- vs. terrestrial contamination) could not be identified. We have recently measured the carbon isotopic ratios of these amino acids to determine their origin, leading to the first detection of a coetary amino acid.