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Sample records for active ethyl acetate

  1. Ethyl acetate

    Integrated Risk Information System (IRIS)

    Ethyl acetate ; CASRN 141 - 78 - 6 Human health assessment information on a chemical substance is included in the IRIS database only after a comprehensive review of toxicity data , as outlined in the IRIS assessment development process . Sections I ( Health Hazard Assessments for Noncarcinogenic Eff

  2. Screening of Methanol Extract and Ethyl Acetate Fraction of Abies webbiana Lindl. for Neuropharmacological Activities

    PubMed Central

    Parkash, O.; Kumar, D.; Kumar, S.

    2015-01-01

    Despite a long traditional of use of Abies webbiana Lindl. (Talispatra; family-Pinaceae) in the treatment of mental disorders, the plant has not been investigated systematically to validate its traditional claims. Thus, the present investigation was undertaken with an objective to investigate neuropharmacological activities of methanol extract of Abies webbiana aerial parts and its ethyl acetate fraction. Properly identified aerial parts were defatted with petroleum ether and then extracted with methanol in a Soxhlet apparatus. Ethyl acetate fraction was prepared by partitioning methanol extract with ethyl acetate using standard procedure. In acute toxicity study, no mortality was observed in animals after oral administration of 2 g/kg dose of methanol extract. The methanol extract (200 or 400 mg/kg, p.o.) and ethyl acetate fraction (25 or 50 mg/kg, p.o.) were evaluated for antianxiety, anticonvulsant, antidepressant, sedative, antistress and analgesic activities using well established models. The methanol extract and ethyl acetate fraction of Abies webbiana aerial parts exhibited significant antianxiety, anticonvulsant, antidepressant, sedative, antistress and analgesic activities with respect to control. Preliminary phytochemical screening showed presence of flavonoids in bioactive ethyl acetate fraction of Abies webbiana aerial parts. It is finally concluded that flavonoids are the bioactive constituents responsible for most of neuropharmacological activities of Abies webbiana. PMID:26798167

  3. Screening of Methanol Extract and Ethyl Acetate Fraction of Abies webbiana Lindl. for Neuropharmacological Activities.

    PubMed

    Parkash, O; Kumar, D; Kumar, S

    2015-01-01

    Despite a long traditional of use of Abies webbiana Lindl. (Talispatra; family-Pinaceae) in the treatment of mental disorders, the plant has not been investigated systematically to validate its traditional claims. Thus, the present investigation was undertaken with an objective to investigate neuropharmacological activities of methanol extract of Abies webbiana aerial parts and its ethyl acetate fraction. Properly identified aerial parts were defatted with petroleum ether and then extracted with methanol in a Soxhlet apparatus. Ethyl acetate fraction was prepared by partitioning methanol extract with ethyl acetate using standard procedure. In acute toxicity study, no mortality was observed in animals after oral administration of 2 g/kg dose of methanol extract. The methanol extract (200 or 400 mg/kg, p.o.) and ethyl acetate fraction (25 or 50 mg/kg, p.o.) were evaluated for antianxiety, anticonvulsant, antidepressant, sedative, antistress and analgesic activities using well established models. The methanol extract and ethyl acetate fraction of Abies webbiana aerial parts exhibited significant antianxiety, anticonvulsant, antidepressant, sedative, antistress and analgesic activities with respect to control. Preliminary phytochemical screening showed presence of flavonoids in bioactive ethyl acetate fraction of Abies webbiana aerial parts. It is finally concluded that flavonoids are the bioactive constituents responsible for most of neuropharmacological activities of Abies webbiana.

  4. Characterization and Antioxidant Properties of Six Algerian Propolis Extracts: Ethyl Acetate Extracts Inhibit Myeloperoxidase Activity

    PubMed Central

    Boufadi, Yasmina Mokhtaria; Soubhye, Jalal; Riazi, Ali; Rousseau, Alexandre; Vanhaeverbeek, Michel; Nève, Jean; Boudjeltia, Karim Zouaoui; Van Antwerpen, Pierre

    2014-01-01

    Because propolis contains many types of antioxidant compounds such as polyphenols and flavonoids, it can be useful in preventing oxidative damages. Ethyl acetate extracts of propolis from several Algerian regions show high activity by scavenging free radicals, preventing lipid peroxidation and inhibiting myeloperoxidase (MPO). By fractioning and assaying ethyl acetate extracts, it was observed that both polyphenols and flavonoids contribute to these activities. A correlation was observed between the polyphenol content and the MPO inhibition. However, it seems that kaempferol, a flavonoid, contributes mainly to the MPO inhibition. This molecule is in a high amount in the ethyl acetate extract and demonstrates the best efficiency towards the enzyme with an inhibiting concentration at 50% of 4 ± 2 μM. PMID:24514562

  5. 21 CFR 584.200 - Ethyl alcohol containing ethyl acetate.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 6 2013-04-01 2013-04-01 false Ethyl alcohol containing ethyl acetate. 584.200... Ethyl alcohol containing ethyl acetate. The feed additive ethyl alcohol containing ethyl acetate meets the requirement of 27 CFR 21.62, being not less than 92.5 percent ethyl alcohol, each 100...

  6. 21 CFR 584.200 - Ethyl alcohol containing ethyl acetate.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 6 2014-04-01 2014-04-01 false Ethyl alcohol containing ethyl acetate. 584.200... Ethyl alcohol containing ethyl acetate. The feed additive ethyl alcohol containing ethyl acetate meets the requirement of 27 CFR 21.62, being not less than 92.5 percent ethyl alcohol, each 100...

  7. 21 CFR 584.200 - Ethyl alcohol containing ethyl acetate.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 6 2012-04-01 2012-04-01 false Ethyl alcohol containing ethyl acetate. 584.200... Ethyl alcohol containing ethyl acetate. The feed additive ethyl alcohol containing ethyl acetate meets the requirement of 27 CFR 21.62, being not less than 92.5 percent ethyl alcohol, each 100...

  8. 21 CFR 584.200 - Ethyl alcohol containing ethyl acetate.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 6 2011-04-01 2011-04-01 false Ethyl alcohol containing ethyl acetate. 584.200... Ethyl alcohol containing ethyl acetate. The feed additive ethyl alcohol containing ethyl acetate meets the requirement of 27 CFR 21.62, being not less than 92.5 percent ethyl alcohol, each 100...

  9. 21 CFR 584.200 - Ethyl alcohol containing ethyl acetate.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Ethyl alcohol containing ethyl acetate. 584.200... Ethyl alcohol containing ethyl acetate. The feed additive ethyl alcohol containing ethyl acetate meets the requirement of 27 CFR 21.62, being not less than 92.5 percent ethyl alcohol, each 100...

  10. Antifungal and antioxidant activity of Crassocephalum bauchiense (Hutch.) Milne-Redh ethyl acetate extract and fractions (Asteraceae)

    PubMed Central

    2014-01-01

    Background Crassocephalum bauchiense is a flowering plant, found in the West Region of Cameroon. Previous studied has highlighted the antibacterial and the dermal toxicological safety as well as the immunomodulatory activities of the ethyl acetate extract of its dry leaves. As an extension of the previous researches, the current work has been undertaken to evaluate the in vitro antifungal and antioxidant activities of C. bauchiense dried leaves ethyl acetate extract and fractions. Methods The extract was obtained by maceration in ethyl acetate and further fractionated into six fractions labeled F1 to F6 by flash chromatography. The antifungal activity of the extract and fractions against yeasts and dermatophytes was evaluated using broth microdilution method. Antioxidant activity was evaluated using 2,2-diphenyl-1-picrylhydrazyl (DPPH), nitric oxide (NO) and β-carotene - linoleic acid assays. Results The extract (MIC = 0.125 - 4 mg/ml) was found to be more active on dermatophytes and yeasts compared to the fractions. The ethyl acetate extract and fractions exhibited strong scavenging activity on DPPH (CI50 = 28.57 - 389.38 μg/ml). The fractions F3 and F6 expressed best antioxidant activity on DPPH radicals compared to the crude extract. Conclusion The results of these findings clearly showed that C. bauchiense ethyl acetate extract has a significant antifungal and antioxidant activity. It is therefore a source of active compounds that might be used as antifungal and antioxidant agents. PMID:24742210

  11. Anti-hepatoma activities of ethyl acetate extract from Ampelopsis sinica root.

    PubMed

    Wang, Jia-Zhi; Huang, Bi-Sheng; Cao, Yan; Chen, Ke-Li; Li, Juan

    2017-03-13

    Ampelopsis sinica root (ASR) is a known hepatoprotective folk traditional Chinese medicine. The anti‑hepatoma activity of ethyl acetate extract from A. sinica root (ASRE) in vitro and in vivo and its possible mechanism were explored. This study was designed to investigate cytotoxicity by MTT assay, induction of apoptosis via Hoechst 33258 staining, scanning electron microscopy and bivariate flow cytometric analysis (Annexin V-FITC/PI), inflammation and apoptosis related genes expression by RT-PCR and p53 protein expression by immunofluorescence assay in HepG2 cells. Then, the antitumor activity in vivo was detected by hepatoma H22 xenograft tumor in mice. The results showed that ASRE had powerful anti‑hepatoma activity in vitro without obvious toxicity on normal cells and could induce HepG2 cell apoptosis. The mechanism may be associated with downregulation of inflammatory cytokines including cyclooxygenase-2, 5-lipoxygenase and FLAP, increase of the ratio of bax/bcl-2, activation caspase-3 and inhibition of survivin, and increased expression of p53 protein. Furthermore, the HPLC assay showed the main compounds of ASRE were gallic acid, catechin and gallic acid ethyl ester. In animal experiments, ASR ethanol extract decreased the tumor weights of hepatoma H22 tumor-bearing mice. Therefore, ASR may be a potential therapeutic agent in the treatment of hepatocellular carcinoma.

  12. Insecticidal Activity of Ethyl Acetate Extracts from Culture Filtrates of Mangrove Fungal Endophytes

    PubMed Central

    Abraham, Silva; Basukriadi, Adi; Pawiroharsono, Suyanto

    2015-01-01

    In the search for novel potent fungi-derived bioactive compounds for bioinsecticide applications, crude ethyl acetate culture filtrate extracts from 110 mangrove fungal endophytes were screened for their toxicity. Toxicity tests of all extracts against brine shrimp (Artemia salina) larvae were performed. The extracts with the highest toxicity were further examined for insecticidal activity against Spodoptera litura larvae and acetylcholinesterase (AChE) inhibition activity. The results showed that the extracts of five isolates exhibited the highest toxicity to brine shrimp at 50% lethal concentration (LC50) values of 7.45 to 10.24 ppm. These five fungal isolates that obtained from Rhizophora mucronata were identified based on sequence data analysis of the internal transcribed spacer region of rDNA as Aspergillus oryzae (strain BPPTCC 6036), Emericella nidulans (strains BPPTCC 6035 and BPPTCC 6038), A. tamarii (strain BPPTCC 6037), and A. versicolor (strain BPPTCC 6039). The mean percentage of S. litura larval mortality following topical application of the five extracts ranged from 16.7% to 43.3%. In the AChE inhibition assay, the inhibition rates of the five extracts ranged from 40.7% to 48.9%, while eserine (positive control) had an inhibition rate of 96.8%, at a concentration of 100 ppm. The extracts used were crude extracts, so their potential as sources of AChE inhibition compounds makes them likely candidates as neurotoxins. The high-performance liquid chromatography profiles of the five extracts differed, indicating variations in their chemical constituents. This study highlights the potential of culture filtrate ethyl acetate extracts of mangrove fungal endophytes as a source of new potential bioactive compounds for bioinsecticide applications. PMID:26190921

  13. Insecticidal Activity of Ethyl Acetate Extracts from Culture Filtrates of Mangrove Fungal Endophytes.

    PubMed

    Abraham, Silva; Basukriadi, Adi; Pawiroharsono, Suyanto; Sjamsuridzal, Wellyzar

    2015-06-01

    In the search for novel potent fungi-derived bioactive compounds for bioinsecticide applications, crude ethyl acetate culture filtrate extracts from 110 mangrove fungal endophytes were screened for their toxicity. Toxicity tests of all extracts against brine shrimp (Artemia salina) larvae were performed. The extracts with the highest toxicity were further examined for insecticidal activity against Spodoptera litura larvae and acetylcholinesterase (AChE) inhibition activity. The results showed that the extracts of five isolates exhibited the highest toxicity to brine shrimp at 50% lethal concentration (LC50) values of 7.45 to 10.24 ppm. These five fungal isolates that obtained from Rhizophora mucronata were identified based on sequence data analysis of the internal transcribed spacer region of rDNA as Aspergillus oryzae (strain BPPTCC 6036), Emericella nidulans (strains BPPTCC 6035 and BPPTCC 6038), A. tamarii (strain BPPTCC 6037), and A. versicolor (strain BPPTCC 6039). The mean percentage of S. litura larval mortality following topical application of the five extracts ranged from 16.7% to 43.3%. In the AChE inhibition assay, the inhibition rates of the five extracts ranged from 40.7% to 48.9%, while eserine (positive control) had an inhibition rate of 96.8%, at a concentration of 100 ppm. The extracts used were crude extracts, so their potential as sources of AChE inhibition compounds makes them likely candidates as neurotoxins. The high-performance liquid chromatography profiles of the five extracts differed, indicating variations in their chemical constituents. This study highlights the potential of culture filtrate ethyl acetate extracts of mangrove fungal endophytes as a source of new potential bioactive compounds for bioinsecticide applications.

  14. Antihyperlipidemic Activity of the Ethyl-acetate Fraction of Stereospermum Suaveolens in Streptozotocin-induced Diabetic Rats

    PubMed Central

    Thirumalaisamy, Balasubramanian; Prabhakaran, Senthilkumar Gnanavadevel; Marimuthu, Karthikeyan; Chatterjee, Tapan Kumar

    2013-01-01

    Objectives: Dyslipidemia in diabetes mellitus is a significant risk factor for the development of cardiovascular complications. The aim of this study was to evaluate the effect of the ethyl-acetate fraction of an ethanolic extract from Streospermum suaveolens on lipid metabolism in streptozotocin (STZ)-induced diabetic rats. Methods: Diabetes was induced by intraperitonial injection of STZ (50 mg/kg). Diabetic rats were treated with an ethyl-acetate fraction orally at doses of 200 and 400 mg/kg daily for 14 days. On the 15th day, serum lipid profiles, such as total cholesterol (TC), triglycerides (TG), low-density lipoprotein (LDL), and high-density lipoprotein (HDL), were estimated in experimental rats. The atherogenic (AI) and the coronary risk (CRI) indices were also evaluated. Results: The ethyl-acetate fraction at doses of 200 and 400 mg/kg significantly (P< 0.001) and dose-dependently reduced serum cholesterol, triglycerides and LDL, but increased HDL towards near normal levels as compared to diabetic control rats. The fraction also significantly (P< 0.001) lowered the atherogenic index (AI) and coronary risk index (CAI) in a dose-dependent manner. Conclusion: The present study demonstrated that the ethyl-acetate fraction of Stereospermum suaveolens exhibits a potent antihyperlipidemic activity in hyperglycemic rats and suggests that the plant may have therapeutic value in treating the diabetic complication of hyperlipidemia. PMID:25780672

  15. Antidiarrhoeal activity of the ethyl acetate extract of Baphia nitida (Papilionaceae).

    PubMed

    Adeyemi, O O; Akindele, A J

    2008-03-28

    In our search for plants useful in the treatment of diarrhoea, we investigated the ethyl acetate extract of Baphia nitida (BN) using intestinal transit, enteropooling and gastric emptying tests in mice and rats. In the castor oil intestinal transit test, BN produced a significant (P<0.05) dose dependent decrease in propulsion with peristaltic index (PI) values of 56.85+/-6.76, 36.84+/-3.04 and 31.98+/-2.60%, respectively at doses of 100, 200 and 400mg/kg vs. 89.33+/-6.28% for control. The effect at 400mg/kg was significantly lower than that of morphine, 10mg/kg, s.c. (20.29+/-3.78%), and was antagonized by isosorbide dinitrate, IDN (150mg/kg, p.o.) but not by yohimbine (1mg/kg, s.c.). This effect was not potentiated by atropine (1mg/kg, s.c.). In the castor oil-induced diarrhoea test, BN produced a significant increase in onset of diarrhoea (103.40+/-8.74, 138.80+/-17.04 and 174.8+/-29.04min, 100 to 400mg/kg, vs. 47.60+/-8.76min for control and 226.10+/-12.57min for morphine). The severity of diarrhoea (diarrhoea score) was dose dependently reduced (19.00+/-2.26, 17.04+/-1.89, 15.00+/-2.05, 100 to 400mg/kg, vs. 31.40+/-2.11 for control and 7.7+/-2.2 for morphine). This effect was not antagonized by IDN or yohimbine. The effect on severity was, however, potentiated by atropine. BN also reduced the number and weight of wet stools but did not have any significant effect on intestinal fluid accumulation and gastric emptying. Results obtained suggest that the ethyl acetate extract of Baphia nitida is endowed with antidiarrhoeal activity possibly mediated by interference with the l-arginine nitric oxide pathway and synergistic with antagonistic action on muscarinic receptors.

  16. Antibacterial Activity of the Isolation Ethyl Acetate-Soluble Extract Noni Fruit (Morindra citrifolia L.) against Meat Bacterial Decay

    NASA Astrophysics Data System (ADS)

    Nugraheni, E. R.; Nurrakhman, M. B. E.; Munawaroh, H.; Saputri, L.

    2017-02-01

    Noni (Morindra citrifolia L.) is native to Indonesia which have medicinal properties. One of them as an antibacterial. This study aims to determine the antibacterial activity of isolates from the ethanol extract noni fruit to bacterial decay meat is Bacillus licheniformis, Klebsiella pneumonia, Bacillus alvei, Acinetobacter calcoaceticus, and Staphylococcus saprophyticus. The extraction process using the maceration method, and then made a partition by centrifugation ethyl acetate. Soluble part partition showed bacterial growth inhibition activity of the strong to very strong. Furthermore, the ethyl acetate soluble partition on preparative thin layer chromatography produced 5 isolates. Isolates obtained antibacterial activity test performed with a concentration of 20% and 30%. The results of antibacterial test against bacteria test isolates, showing isolates A can not inhibit the growth of bacteria, isolates B and C have medium activity and strong, isolates D and E isolates have activity against bacteria that were tested. MIC and MBC test results showed that the isolates B gives an inhibitory effect (bacteriostatic) against all bacteria. Content analysis of compounds by TLC using the reagents cerium (IV) sulfate indicates a phenol group. Isolates B contains a major compound which can be used as an antibacterial candidate in food preservation replace chemical preservatives.

  17. Manufacturing Ethyl Acetate From Fermentation Ethanol

    NASA Technical Reports Server (NTRS)

    Rohatgi, Naresh K.; Ingham, John D.

    1991-01-01

    Conceptual process uses dilute product of fermentation instead of concentrated ethanol. Low-concentration ethanol, extracted by vacuum from fermentation tank, and acetic acid constitutes feedstock for catalytic reaction. Product of reaction goes through steps that increases ethyl acetate content to 93 percent by weight. To conserve energy, heat exchangers recycle waste heat to preheat process streams at various points.

  18. Antibacterial activity of Pyrrosia petiolosa ethyl acetate extract against Staphylococcus aureus by decreasing hla and sea virulence genes.

    PubMed

    Song, Liju; Cao, Mei; Chen, Chong; Qi, Panpan; Li, Ningzhe; Wu, Daoyan; Peng, Jingshan; Wang, Xuege; Zhang, Mao; Hu, Guoku; Zhao, Jian

    2017-06-01

    The aim of this study was to explore the antibacterial activity of Pyrrosia petiolosa ethyl acetate extract (PPEAE) against Staphylococcus aureus in vitro and analyse its chemical components by gas chromatograph-mass spectrometry. The results of anti-microbial assay revealed that PPEAE had strong inhibitory activity against S .aureus, with MIC and MBC of 7.8 and 15.6 mg/mL, respectively. The transcriptional levels of hla and sea were reduced to 14.33 and 46.39% at the MIC compared to the control. Analysing test result exhibited that eugenol made a great contribution to antibacterial activity. This experiment indicated that PPEAE had prominent antibacterial activity against S. aureus.

  19. 21 CFR 173.228 - Ethyl acetate.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 3 2014-04-01 2014-04-01 false Ethyl acetate. 173.228 Section 173.228 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) SECONDARY DIRECT FOOD ADDITIVES PERMITTED IN FOOD FOR HUMAN CONSUMPTION Solvents, Lubricants, Release Agents and...

  20. Evaluation of Antibacterial, Antineoplastic, and Immunomodulatory Activity of Paullinia cupana Seeds Crude Extract and Ethyl-Acetate Fraction.

    PubMed

    Carvalho, Lidiane Vasconcelos do Nascimento; Cordeiro, Marina Ferraz; E Lins, Thiago Ubiratan Lins; Sampaio, Maria Clara Pinheiro Duarte; de Mello, Gabriela Souto Vieira; da Costa, Valécia de Cassia Mendonça; Marques, Leila Larisa Medeiros; Klein, Traudi; de Mello, João Carlos Palazzo; Cavalcanti, Isabella Macário Ferro; Pitta, Ivan da Rocha; Galdino da Rocha Pitta, Maira; Rêgo, Moacyr Jesus Barreto de Melo

    2016-01-01

    Paullinia cupana (Guarana) is a native plant of Amazon region that has very traditional importance. Its seeds are rich in bioactive compounds, including tannins, which exhibit relevant properties. Objective. This study aimed to evaluate antibacterial, antineoplastic, and immunomodulatory activity of P. cupana seeds crude extract (CE) and ethyl-acetate fraction (EAF). Methods. Antibacterial activity was evaluated by determination of minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC). Antineoplastic activity was evaluated by MTT assays in hepatocellular carcinoma (HepG2), breast adenocarcinoma (MCF-7), ductal carcinoma (T47-D), non-Hodgkin's B cell lymphoma (Toledo), T cell leukemia (Jukart), and Acute Leukemia (HL-60) cell lines. BALB/c mice splenocytes were treated to assess IFN-γ, IL-6, IL-17, and IL-10 levels by sandwich ELISA. Results. CE and EAF were not toxic to peripheral blood cells and splenocytes. CE and EAF fractions showed a bacteriostatic activity (MIC = 250 μg/mL) and presented IC50 values of 70.25 μg/mL and 61.18 μg/mL in HL-60 leukemia cell line. All cytokines evaluated had their levels reduced after treatment, following dose-response model. Discussion and Conclusion. Different biological activities were observed for both CE and EAF, suggesting P. cupana as a source of bioactive substances, especially tannins that may be used for several diseases treatments.

  1. Antitumor Activities of Ethyl Acetate Extracts from Selaginella doederleinii Hieron In Vitro and In Vivo and Its Possible Mechanism

    PubMed Central

    Li, Juan; Zhao, Ping; Ma, Wen-tao; Feng, Xie-he; Chen, Ke-li

    2015-01-01

    The antitumor activities of ethyl acetate extracts from Selaginella doederleinii Hieron (SD extracts) in vitro and in vivo and its possible mechanism were investigated. HPLC method was developed for chemical analysis. SD extracts were submitted to 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay on different cells, flow cytometry, and RT-PCR analysis using HepG2 cell and antitumor activity in vivo using H-22 xenograft tumor mice. Six biflavonoids from SD extracts were submitted to molecular docking assay. The results showed that SD extracts had considerable antitumor activity in vitro and in vivo without obvious toxicity on normal cells and could induce cell apoptosis. The mechanisms of tumorigenesis and cell apoptosis induced by SD extracts may be associated with decreasing the ratio of bcl-2 and bax mRNA level, activating caspase-3, suppressing survivin, and decreasing the gene expression of COX-2, 5-LOX, FLAP, and 12-LOX mRNA. The main active component in SD extracts is biflavonoids and some exhibited strong interactions with COX-2, 5-LOX, 12-LOX, and 15-LOX. These results offering evidence of possible mechanisms of SD extracts suppress cell proliferation and promote apoptosis and provide the molecular theoretical basis of clinical application of S. doederleinii for cancer therapy. PMID:25866543

  2. Evaluation of Antibacterial, Antineoplastic, and Immunomodulatory Activity of Paullinia cupana Seeds Crude Extract and Ethyl-Acetate Fraction

    PubMed Central

    Carvalho, Lidiane Vasconcelos do Nascimento; Cordeiro, Marina Ferraz; e Lins, Thiago Ubiratan Lins; Sampaio, Maria Clara Pinheiro Duarte; de Mello, Gabriela Souto Vieira; da Costa, Valécia de Cassia Mendonça; Marques, Leila Larisa Medeiros; Klein, Traudi; de Mello, João Carlos Palazzo; Cavalcanti, Isabella Macário Ferro; Pitta, Ivan da Rocha

    2016-01-01

    Paullinia cupana (Guarana) is a native plant of Amazon region that has very traditional importance. Its seeds are rich in bioactive compounds, including tannins, which exhibit relevant properties. Objective. This study aimed to evaluate antibacterial, antineoplastic, and immunomodulatory activity of P. cupana seeds crude extract (CE) and ethyl-acetate fraction (EAF). Methods. Antibacterial activity was evaluated by determination of minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC). Antineoplastic activity was evaluated by MTT assays in hepatocellular carcinoma (HepG2), breast adenocarcinoma (MCF-7), ductal carcinoma (T47-D), non-Hodgkin's B cell lymphoma (Toledo), T cell leukemia (Jukart), and Acute Leukemia (HL-60) cell lines. BALB/c mice splenocytes were treated to assess IFN-γ, IL-6, IL-17, and IL-10 levels by sandwich ELISA. Results. CE and EAF were not toxic to peripheral blood cells and splenocytes. CE and EAF fractions showed a bacteriostatic activity (MIC = 250 μg/mL) and presented IC50 values of 70.25 μg/mL and 61.18 μg/mL in HL-60 leukemia cell line. All cytokines evaluated had their levels reduced after treatment, following dose-response model. Discussion and Conclusion. Different biological activities were observed for both CE and EAF, suggesting P. cupana as a source of bioactive substances, especially tannins that may be used for several diseases treatments. PMID:28053639

  3. Pallidol hexa­acetate ethyl acetate monosolvate

    PubMed Central

    Mao, Qinyong; Taylor, Dennis K.; Ng, Seik Weng; Tiekink, Edward R. T.

    2013-01-01

    The entire mol­ecule of pallidol hexa­acetate {systematic name: (±)-(4bR,5R,9bR,10R)-5,10-bis­[4-(acet­yloxy)phen­yl]-4b,5,9b,10-tetra­hydro­indeno­[2,1-a]indene-1,3,6,8-tetrayl tetra­acetate} is completed by the application of twofold rotational symmetry in the title ethyl acetate solvate, C40H34O12·C4H8O2. The ethyl acetate mol­ecule was highly disordered and was treated with the SQUEEZE routine [Spek (2009 ▶). Acta Cryst. D65, 148–155]; the crystallographic data take into account the presence of the solvent. In pallidol hexa­acetate, the dihedral angle between the fused five-membered rings (r.m.s. deviation = 0.100 Å) is 54.73 (6)°, indicating a significant fold in the mol­ecule. Significant twists between residues are also evident as seen in the dihedral angle of 80.70 (5)° between the five-membered ring and the pendent benzene ring to which it is attached. Similarly, the acetate residues are twisted with respect to the benzene ring to which they are attached [C—O(carb­oxy)—C—C torsion angles = −70.24 (14), −114.43 (10) and −72.54 (13)°]. In the crystal, a three-dimensional architecture is sustained by C—H⋯O inter­actions which encompass channels in which the disordered ethyl acetate mol­ecules reside. PMID:24046702

  4. Nitrosation of glycine ethyl ester and ethyl diazoacetate to give the alkylating agent and mutagen ethyl chloro(hydroximino)acetate.

    PubMed

    Zhou, Lin; Haorah, James; Chen, Sheng C; Wang, Xiaojie; Kolar, Carol; Lawson, Terence A; Mirvish, Sidney S

    2004-03-01

    Whereas nitrosation of secondary amines produces nitrosamines, amino acids with primary amino groups and glycine ethyl ester were reported to react with nitrite to give unidentified agents that alkylated 4-(p-nitrobenzyl)pyridine to produce purple dyes and be direct mutagens in the Ames test. We report here that treatment of glycine ethyl ester at 37 degrees C with excess nitrite acidified with HCl, followed by ether extraction, gave 30-40% yields of a product identified as ethyl chloro(hydroximino)acetate [ClC(=NOH)COOEt, ECHA] and a 9% yield of ethyl chloroacetate. The ECHA was identical to that synthesized by a known method from ethyl acetoacetate, strongly alkylated nitrobenzylpyridine, and may have arisen by N-nitrosation of glycine ethyl ester to give ethyl diazoacetate, which was C-nitrosated and reacted with chloride to give ECHA. Nitrosation of ethyl diazoacetate also yielded ECHA. Ethyl nitroacetate was not an intermediate as its nitrosation did not produce ECHA. ECHA reacted with aniline to give ethyl (hydroxamino)(phenylimino)acetate [PhN=C(NHOH)CO2Et]. This product was different from ethyl [(phenylamino)carbonyl]carbamate [PhNHC(=O)NHCO2Et], which was synthesized by reacting ethyl isocyanatoformate (OCN.CO2Et) with aniline. ECHA reacted with guanosine to give a derivative, which may have been a guanine-C(=NOH)CO2Et derivative. ECHA showed moderate toxicity and weak but significant mutagenicity without activation in Salmonella typhimurium TA-100 (mean, 1.31 x control value for 12-18 microg/plats) and for V79 mammalian cells (1.5-1.7 x control value for 60-100 microM). In conclusion, gastric nitrosation of glycine derivatives such as peptides with a N-terminal glycine might produce ECHA analogues that alkylate bases of gastric mucosal DNA and thereby initiate gastric cancer.

  5. Activation of apoptosis by ethyl acetate fraction of ethanol extract of Dianthus superbus in HepG2 cell line.

    PubMed

    Yu, Jian-Qing; Yin, Yan; Lei, Jia-Chuan; Zhang, Xiu-Qiao; Chen, Wei; Ding, Cheng-Li; Wu, Shan; He, Xiao-Yu; Liu, Yan-Wen; Zou, Guo-Lin

    2012-02-01

    Dianthus superbus L. is commonly used as a traditional Chinese medicine. We recently showed that ethyl acetate fraction (EE-DS) from ethanol extract of D. superbus exhibited the strongest antioxidant and cytotoxic activities. In this study, we examined apoptosis of HepG2 cells induced by EE-DS, and the mechanism underlying apoptosis was also investigated. Treatment of HepG2 cells with EE-DS (20-80 μg/ml) for 48 h led to a significant dose-dependent increase in the percentage of cells in sub-G1 phase by analysis of the content of DNA in cells, and a large number of apoptotic bodies containing nuclear fragments were observed in cells treated with 80 μg/ml of EE-DS for 24 h by using Hoechst 33258 staining. These data show that EE-DS can induce apoptosis of HepG2 cells. Immunoblot analysis showed that EE-DS significantly suppressed the expressions of Bcl-2 and NF-κB. Treatment of cells with EE-DS (80 μg/ml) for 48 h resulted in significant increase of cytochrome c in the cytosol, which indicated cytochrome c release from mitochondria. Activation of caspase-9 and -3 were also determined when the cells treated with EE-DS. The results suggest that apoptosis of HepG2 cells induced by EE-DS could be through the mitochondrial intrinsic pathway. High performance liquid chromatography (HPLC) data showed that the composition of EE-DS is complicated. Further studies are needed to find the effective constituents of EE-DS.

  6. Identification of Pyrogallol in the Ethyl Acetate-Soluble Part of Coffee as the Main Contributor to Its Xanthine Oxidase Inhibitory Activity.

    PubMed

    Honda, Sari; Masuda, Toshiya

    2016-10-10

    In this study, ethyl acetate-soluble parts of hot-water extracts from roasted coffee beans were found to demonstrate potent xanthine oxidase (XO) inhibition. The XO inhibitory activities and chlorogenic lactone contents (chlorogenic lactones have previously been identified as XO inhibitors in roast coffee) were measured for ethyl acetate-soluble parts prepared from coffee beans roasted to three different degrees. Although chlorogenic lactone contents decreased with higher degrees of roasting, the XO inhibitory activity did not decrease. These data led us to investigate new potent inhibitors present in these ethyl acetate-soluble extracts. Repeated assay-guided purifications afforded a highly potent XO inhibitor, which was eluted before chlorogenic lactones via medium-pressure chromatography using an octadecylsilica gel column. The obtained inhibitor was identified as pyrogallol (1,2,3-trihydroxybenzene), which had an IC50 of 0.73 μmol L(-1), much stronger than that of other related polyphenolic compounds. Quantitative analysis of pyrogallol and chlorogenic lactones revealed that pyrogallol (at concentrations of 33.9 ± 4.2 nmol mL(-1) in light roast coffee and 39.4 ± 3.9 nmol mL(-1) in dark roast coffee) was the main XO inhibitor in hot-water extracts of roasted coffee beans (i.e., drinking coffee).

  7. Antidiabetic Activity of Self Nanoemulsifying Drug Delivery System from Bay Leaves (Eugenia polyantha Wight) Ethyl Acetate Fraction

    NASA Astrophysics Data System (ADS)

    Prihapsara, F.; Harini, M.; Widiyani, T.; Artanti, A. N.; Ani, I. L.

    2017-02-01

    Insulin resistance is caused by inability of target tissues to insulin response. Bay leaves (Eugenia polyantha Wight) fraction or extract have been used for the treatment of antidibetic mellitus type-2 resistance insulin (ADMRI) but it has low solubility and bioavailability. To overcome these problems, ethyl acetate fraction of bay leaves was formulated into self nanoemulsifying drug delivery system (SNEDDS) using Virgin Coconut Oil (VCO) as a carrier oil. This study aims to produce nanoherbal medicine, determine effect of nanoherbal preparation derived from bay leaves as an anti-ADMRI. The results showed that the optimum SNEDDS formula was tween 80 : PEG 400 : Virgin Coconut Oil (30% : 60% : 10%) in 5 mL. It has emulsification time 13.00 seconds with the average of droplet size value 84.5 nanometer and zeta potential value ± 0.2 mV. Morphological observation showed the nanoemulsion particles has spherical shaped and stable in different pH media. Hypoglycaemic effect of single dose metformin, SNEDDS, combination a-half dose of SNEEDS with metformin value is 28.3%; 15.6%; 34.6% respectively.

  8. Kinetics of Ethyl Acetate Synthesis Catalyzed by Acidic Resins

    ERIC Educational Resources Information Center

    Antunes, Bruno M.; Cardoso, Simao P.; Silva, Carlos M.; Portugal, Ines

    2011-01-01

    A low-cost experiment to carry out the second-order reversible reaction of acetic acid esterification with ethanol to produce ethyl acetate is presented to illustrate concepts of kinetics and reactor modeling. The reaction is performed in a batch reactor, and the acetic acid concentration is measured by acid-base titration versus time. The…

  9. Ethyl acetate-n-butanol gradient solvent system for high-speed countercurrent chromatography to screen bioactive substances in okra.

    PubMed

    Ying, Hao; Jiang, Heyuan; Liu, Huan; Chen, Fangjuan; Du, Qizhen

    2014-09-12

    High-speed countercurrent chromatographic separation (HSCCC) possesses the property of zero-loss of sample, which is very useful for the screening of bioactive components. In the present study, the ethyl acetate-n-butanol gradient HSCCC solvent system composed of n-hexane-ethyl acetate-n-butanol-water was investigated for the screening of bioactive substances. To screen the antiproliferative compounds in okra extract, we used the stationary phase ethyl acetate-n-butanol-water (1:1:10) as the stationary phase, and eluted the antiproliferative components by 6-steps of gradient using mobile phases n-hexane-ethyl acetate (1:2), n-hexane-ethyl acetate (1:4), n-hexane-ethyl acetate (0:4), n-butanol-ethyl acetate (1:4) n-butanol-ethyl acetate (1:2), n-butanol-ethyl acetate (2:2), and n-butanol-ethyl acetate (2:1). The fractions collected from HSCCC separation with the gradient solvent system were assayed for antiproliferative activity against cancer cells. Bioactive components were identified: a major anti-cancer compound, 4'-hydroxy phenethyl trans-ferulate, with middle activity, and a minor anti-cancer compound, carolignan, with strong activity. The result shows that the gradient solvent system is potential for the screening of bioactive compounds from natural products.

  10. Cytotoxic constituents of ethyl acetate fraction from Dianthus superbus.

    PubMed

    Ding, Chengli; Zhang, Wu; Li, Jie; Lei, Jiachuan; Yu, Jianqing

    2013-01-01

    The ethyl acetate fraction (EE-DS) from Dianthus superbus was found to possess the cytotoxic activity against cancer cells in previous study. To investigate cytotoxic constituents, the bioassay-guided isolation of compounds from EE-DS was performed. Two dianthramides (1 and 2), three flavonoids (3-5), two coumarins (6 and 7) and three other compounds (8-10) were obtained. Structures of isolated compounds were identified by spectroscopic analysis. Cytotoxicity of the compounds against HepG2 cells was evaluated. Compound 1 showed the strongest cytotoxicity, compounds 10, 4, 3 and 5 had moderate cytotoxicity.

  11. Cognitive enhancing and antioxidant activity of ethyl acetate soluble fraction of the methanol extract of Hibiscus rosa sinensis in scopolamine-induced amnesia

    PubMed Central

    Nade, Vandana S.; Kanhere, Sampat V.; Kawale, Laxman A.; Yadav, Adhikrao V.

    2011-01-01

    Objective: The objective of the present study was to evaluate the cognitive enhancing and antioxidant activity of Hibiscus rosa sinensis. Materials and Methods: The learning and memory was impaired by administration of scopolamine (1 mg/kg, i.p.) in mice which is associated with altered brain oxidative status. The object recognition test (ORT) and passive avoidance test (PAT) were used to assess cognitive enhancing activity. Animals were treated with an ethyl acetate soluble fraction of the methanol extract of H. sinensis (25, 50 and 100 mg/kg, p.o). Results: The ethyl acetate soluble fraction of the methanol extract of H. sinensis (EASF) attenuated amnesia induced by scopolamine and aging. The discrimination index (DI) was significantly decreased in the aged and scopolamine group in ORT. Pretreatment with EASF significantly increased the DI. In PAT, scopolamine-treated mice exhibited significantly shorter step-down latencies (SDL). EASF treatment showed a significant increase in SDL in young, aged as well as in scopolamine-treated animals. The biochemical analysis of brain revealed that scopolamine treatment increased lipid peroxidation and decreased levels of superoxide dismutase (SOD) and glutathione reductase (GSH). Administration of extract significantly reduced LPO and reversed the decrease in brain SOD and GSH levels. The administration of H. sinensis improved memory in amnesic mice and prevented the oxidative stress associated with scopolamine. The mechanism of such protection of H. sinensis may be due to augmentation of cellular antioxidants. Conclusion: The results of the present study suggested that H. sinensis had a protective role against age and scopolamine-induced amnesia, indicating its utility in management of cognitive disorders. PMID:21572646

  12. Fragrance material review on ethyl phenyl carbinyl acetate.

    PubMed

    McGinty, D; Letizia, C S; Api, A M

    2012-09-01

    A toxicologic and dermatologic review of ethyl phenyl carbinyl acetate when used as a fragrance ingredient is presented. Ethyl phenyl carbinyl acetate is a member of the fragrance structural group Aryl Alkyl Alcohol Simple Acid Esters (AAASAE). The AAASAE fragrance ingredients are prepared by reacting an aryl alkyl alcohol with a simple carboxylic acid (a chain of 1-4 carbons) to generate formate, acetate, propionate, butyrate, isobutyrate and carbonate esters. This review contains a detailed summary of all available toxicology and dermatology papers that are related to this individual fragrance ingredient and is not intended as a stand-alone document. Available data for ethyl phenyl carbinyl acetate were evaluated, then summarized, and includes: physical properties; acute toxicity; skin irritation; and skin sensitization data. A safety assessment of the entire AAASAE will be published simultaneously with this document; please refer to Belsito et al. (2012) for an overall assessment of the safe use of this material and all AAASAE in fragrances.

  13. Fragrance material review on 2-(p-tolyloxy)ethyl acetate.

    PubMed

    McGinty, D; Letizia, C S; Api, A M

    2012-09-01

    A toxicologic and dermatologic review of 2-(p-tolyloxy)ethyl acetate when used as a fragrance ingredient is presented. 2-(p-tolyloxy)ethyl acetate is a member of the fragrance structural group aryl alkyl alcohol simple acid esters (AAASAE). The AAASAE fragrance ingredients are prepared by reacting an aryl alkyl alcohol with a simple carboxylic acid (a chain of 1-4 carbons) to generate formate, acetate, propionate, butyrate, isobutyrate and carbonate esters. This review contains a detailed summary of all available toxicology and dermatology papers that are related to this individual fragrance ingredient and is not intended as a stand-alone document. Available data for 2-(p-tolyloxy)ethyl acetate were evaluated, then summarized, and includes physical properties data. A safety assessment of the entire AAASAE will be published simultaneously with this document. Please refer to Belsito et al. (2012) for an overall assessment of the safe use of this material and all AAASAE in fragrances.

  14. Evaluation of Antiradical and Anti-Inflammatory Activities of Ethyl Acetate and Butanolic Subfractions of Agelanthus dodoneifolius (DC.) Polhill & Wiens (Loranthaceae) Using Equine Myeloperoxidase and Both PMA-Activated Neutrophils and HL-60 Cells

    PubMed Central

    Boly, Rainatou; Franck, Thierry; Kohnen, Stephan; Lompo, Marius; Guissou, Innocent Pierre; Dubois, Jacques; Serteyn, Didier; Mouithys-Mickalad, Ange

    2015-01-01

    The ethyl acetate and n-butanolic subfractions of Agelanthus dodoneifolius were investigated for their antioxidant and antimyeloperoxidase (MPO) activities. The reactive oxygen species (ROS) generation was assessed by lucigenin-enhanced chemiluminescence (CL) and dichlorofluorescein- (DCF-) induced fluorescence techniques from phorbol myristate acetate- (PMA-) stimulated equine neutrophils and human myeloid cell line HL-60, respectively. In parallel, the effects of the tested subfractions were evaluated on the total MPO release by stimulated neutrophils and on the specific MPO activity by means of immunological assays. The results showed the potent activity of the butanolic subfraction, at least in respect of the chemiluminescence test (IC50 = 0.3 ± 0.1 µg/mL) and the ELISA and SIEFED assays (IC50 = 2.8 ± 1.2 µg/mL and 1.3 ± 1.0 µg/mL), respectively. However, the ethyl acetate subfraction was found to be the most potent in the DCF assay as at the highest concentration, DCF fluorescence intensity decreases of about 50%. Moreover, we demonstrated that the ethyl acetate subfraction was rich in catechin (16.51%) while it was not easy to identify the main compounds in the butanolic subfraction using the UPLC-MS/MS technique. Nevertheless, taken together, our results provide evidence that Agelanthus dodoneifolius subfractions may represent potential sources of natural antioxidants and of antimyeloperoxidase compounds. PMID:25821497

  15. In Vivo Antioxidant and Anti-Skin-Aging Activities of Ethyl Acetate Extraction from Idesia polycarpa Defatted Fruit Residue in Aging Mice Induced by D-Galactose

    PubMed Central

    Jia, Ran-ran; Chen, Fang

    2014-01-01

    Two different concentrations of D-galactose (D-gal) induced organism and skin aging in Kunming mice were used to examine comprehensively the antioxidant and antiaging activities of ethyl acetate extraction (EAE) from Idesia polycarpa defatted fruit residue for the first time. The oxygen radical absorbance capacity (ORAC) of EAE was 13.09 ± 0.11 μmol Trolox equivalents (TE)/mg, which showed EAE had great in vitro free radical scavenging and antioxidant activity. Biochemical indexes and morphological analysis of all tested tissues showed that EAE could effectively improve the total antioxidant capacity (T-AOC) of the antioxidant defense system of the aging mice, enhance the activities of superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GSH-Px) of tissues and serum, increase glutathione (GSH) content and decrease the malondialdehyde (MDA) content, and maintain the skin collagen, elastin, and moisture content. Meanwhile, EAE could effectively attenuate the morphological damage in brain, liver, kidney, and skin induced by D-gal and its effect was not less than that of the well-known L-ascorbic acid (VC) and α-tocopherol (VE). Overall, EAE is a potent natural antiaging agent with great antioxidant activity, which can be developed as a new medicine and cosmetic for the treatment of age-related conditions. PMID:24971146

  16. Effect of preparation method on the surface characteristics and activity of the Pd/OMS-2 catalysts for the oxidation of carbon monoxide, toluene, and ethyl acetate

    NASA Astrophysics Data System (ADS)

    Liu, Lisha; Song, Yong; Fu, Zhidan; Ye, Qing; Cheng, Shuiyuan; Kang, Tianfang; Dai, Hongxing

    2017-02-01

    The cryptomelane-type manganese oxide octahedral molecular sieve (OMS-2)-supported Pd (0.5 wt% Pd/OMS-2-DP, 0.5 wt% Pd/OMS-2-PI, and 0.5 wt% Pd/OMS-2-EX) catalysts were prepared by the deposition-precipitation, pre-incorporation, and ion-exchanging strategies, respectively. It is shown that the preparation method exerted an important effect on the physicochemical property of the sample. Among the OMS-2-supported Pd catalysts, 0.5 wt% Pd/OMS-2-DP possessed the highest surface (Mn2+ + Mn3+)/Mn4+ atomic ratio and the highest surface Pd loading and acid sites. The 0.5 wt% Pd/OMS-2 catalysts outperformed the Pd-free counterpart, among which 0.5 wt% Pd/OMS-2-DP presented the best catalytic activity (T50% and T90% were 25 and 55 °C for CO oxidation, 240 and 285 °C for toluene oxidation, and 160 and 200 °C for ethyl acetate oxidation, respectively). We believe that the high Pd surface loading, high surface atomic ratio of (Mn2+ + Mn3+)/Mn4+, and good low-temperature reducibility, good oxygen mobility, and high acidity were responsible for the excellent performance of the 0.5 wt% Pd/OMS-2-DP catalyst.

  17. Ethyl acetate extract from marine sponge Hyattella cribriformis exhibit potent anticancer activity by promoting tubulin polymerization as evidenced mitotic arrest and induction of apoptosis

    PubMed Central

    Annamalai, Pazhanimuthu; Thayman, Malini; Rajan, Sowmiya; Raman, Lakshmi Sundaram; Ramasubbu, Sankar; Perumal, Pachiappan

    2015-01-01

    Background: Marine sponges are important sources of bioactive compounds. Objective: This study investigated the anticancer properties of Hyattella cribriformis ethyl acetate (EA) fraction in various cancer and normal cell lines. Materials and Methods: anticancer assay was carried out in 15 cell lines to evaluate the anticancer potential of the EA fraction. Impact on cell cycle distribution was determined using flow cytometry. The fraction was investigated for interfering microtubules assembly in both in vitro and cellular assay. Further studies were conducted to determine the fraction induced cell death (apoptosis) using calcein/propidium iodide dual staining, activated caspase-3 and phosphorylation of Bcl-2 protein at Ser70. DNA fragmentation assay was performed to confirm the apoptosis. Results: EA fraction exhibited potent inhibition of cancer cell growth and resulted in 50% growth inhibition (GI50) of 0.27 μg/mL in A673 cell line. Sarcoma (MG-63, Saos-2) and ovarian (SK-OV-3 and OVCAR-3) cancer cell lines also showed superior anticancer activity GI50 of 1.0 μg/mL. Colon and breast cancer cell lines exhibited moderate GI compare other cancer cell lines and normal human lung fibroblast showed GI50 of 15.6 μg/mL. EA fraction showed potent G2/M phase arrest in A673 cell line and induced apoptosis at 48 h exposure. EA fraction promoted microtubule polymerization in tubulin polymerization assay and increased level of polymerized tubulin in the HeLa cells. Fraction induced the activation of caspase-3 and phosphorylation of Bcl-2 anti-apoptotic protein. Fraction induced DNA fragmentation in HeLa cells as evidence of apoptosis. Conclusion: Marine sponge H. cribriformis EA fraction exhibited potent anticancer activity through tubulin polymerization and induction of apoptosis. PMID:25829774

  18. Atmospheric Oxidation Mechanisms for Diethyl Ether and its Oxidation Products, Ethyl Formate and Ethyl Acetate.

    NASA Astrophysics Data System (ADS)

    Orlando, J. J.; Tyndall, G. S.

    2006-12-01

    Carbon-containing compounds are present in the earth's atmosphere as the result of emissions from natural and anthropogenic sources. Their oxidation in the atmosphere, initiated by such oxidants as OH, ozone, and nitrate radicals, leads to potentially harmful secondary pollutants such as ozone, carbonyl species, organic acids and aerosols. Ethers and esters are two classes of compounds that contribute to the complex array of organic compounds found in anthropogenically-influenced air. Additional ester is present as a result of the oxidation of the ethers. In this paper, the oxidation of diethyl ether and its two main oxidation products, ethyl formate and ethyl acetate, are studied over ranges of temperature, oxygen partial pressure, and NOx concentration, using an environmental chamber / FTIR absorption technique. Major end-products (the esters from diethyl ether; organic acids and anhydrides from the esters) are quantified, and these data are interpreted in terms of the chemistry of the various alkoxy and peroxy radicals generated. Emphasis is placed on the effects of chemical activation on the behavior of the alkoxy radicals, as well as on a novel peroxy radical rearrangement that may contribute to the observed products of ether oxidation under some conditions. Finally, the data are used, in conjunction with data on similar species, to provide a general representation of ether and ester oxidation in the atmosphere.

  19. Antiplasmodial Properties and Bioassay-Guided Fractionation of Ethyl Acetate Extracts from Carica papaya Leaves.

    PubMed

    Melariri, Paula; Campbell, William; Etusim, Paschal; Smith, Peter

    2011-01-01

    We investigated the antiplasmodial properties of crude extracts from Carica papaya leaves to trace the activity through bioassay-guided fractionation. The greatest antiplasmodial activity was observed in the ethyl acetate crude extract. C. papaya showed a high selectivity for P. falciparum against CHO cells with a selectivity index of 249.25 and 185.37 in the chloroquine-sensitive D10 and chloroquine-resistant DD2 strains, respectively. Carica papaya ethyl acetate extract was subjected to bioassay-guided fractionation to ascertain the most active fraction, which was purified and identified using high-pressure liquid chromatography (HPLC) and GC-MS (Gas chromatography-Mass spectrometry) methods. Linoleic and linolenic acids identified from the ethyl acetate fraction showed IC(50) of 6.88 μg/ml and 3.58 μg/ml, respectively. The study demonstrated greater antiplasmodial activity of the crude ethyl acetate extract of Carica papaya leaves with an IC(50) of 2.96 ± 0.14 μg/ml when compared to the activity of the fractions and isolated compounds.

  20. Bioactivity of Diterpens from the Ethyl Acetate Extract of Kingiodendron pinnatum Rox. Hams

    PubMed Central

    Javarappa, Komal Kumar; Prasad, Attemode Girijanna Devi; Mahadesh Prasad, AJ; Mane, Chetana

    2016-01-01

    Background: Kingiodendron pinnatum Rox. Hams. is an endangered medicinal plant used in gonorrhoe, catarrhal conditions of genito-urinary and respiratory tracts. The scientific and pharmacological formulation of K. pinnatum has not been established so far though it is being traditionally used by tribes of the region. Objective: P hytochemical screening and identification of the bioactive compounds from the ethyl acetate extract of Kingiodendron pinnatum Rox. Hams. Materials and Methods: Chromatographic separation was carried out by thin layer chromatography and column chromatography. Bio-autography of the column fractioned extract and TLC chromatogram were evaluated in vitro for antibacterial activity. The PTLC, HP TLC were used for crude extract and HPLC, LCMS, FTIR, 1HNMR and 13CNMR were employed for the isolated compound in the ethyl acetate extract of K. pinnatum. Results: Evaluation of solvent system for chromatographic separation revealed that ethyl acetate: petroleum ether in the ratio of 7:2.5 ml was the most appropriate one for the separation of diterpene compounds. The antibacterial bio-autography screening of TLC separated compound showed positive activity with Staphylococcus aureus and negative activity with Escherichia coli. Spectroscopic analysis of the isolated compound from the ethyl acetate extract of K. pinnatum revealed the presence of diterpene compound. Conclusion: It is evident from the present study that the ethyl acetate extract of K. pinnatum is rich in diterpene compounds and having potential antibacterial activity. SUMMARY Novel extraction method for phytochemicls from Kingidendron pinnatum at RTAntibacterial property of diterpens extracted from Kingiodendron pinnatum Rox. Hams aganist S. aureus Abbreviations Used: TLC: Thin Layer Chromatography, PTLC: Preparatory Thin Layer Chromatography, HPTLC: High perormence Thin Layer chromatography, HPLC: High Performance Liquid Chromatography, LC-MS: Liquid chromatography Mass Spectra, FTIR

  1. Wound healing properties of ethyl acetate fraction of Moringa oleifera in normal human dermal fibroblasts

    PubMed Central

    Gothai, Sivapragasam; Arulselvan, Palanisamy; Tan, Woan Sean; Fakurazi, Sharida

    2016-01-01

    Background/Aim: Wounds are the outcome of injuries to the skin that interrupt the soft tissue. Healing of a wound is a complex and long-drawn-out process of tissue repair and remodeling in response to injury. A large number of plants are used by folklore traditions for the treatment of cuts, wounds and burns. Moringa oleifera (MO) is an herb used as a traditional folk medicine for the treatment of various skin wounds and associated diseases. The underlying mechanisms of wound healing activity of ethyl acetate fraction of MO leaves extract are completely unknown. Materials and Methods: In the current study, ethyl acetate fraction of MO leaves was investigated for its efficacy on cell viability, proliferation and migration (wound closure rate) in human normal dermal fibroblast cells. Results: Results revealed that lower concentration (12.5 µg/ml, 25 µg/ml, and 50 µg/ml) of ethyl acetate fraction of MO leaves showed remarkable proliferative and migratory effect on normal human dermal fibroblasts. Conclusion: This study suggested that ethyl acetate fraction of MO leaves might be a potential therapeutic agent for skin wound healing by promoting fibroblast proliferation and migration through increasing the wound closure rate corroborating its traditional use. PMID:27069722

  2. Acetic acid removal from corn stover hydrolysate using ethyl acetate and the impact on Saccharomyces cerevisiae bioethanol fermentation.

    PubMed

    Aghazadeh, Mahdieh; Ladisch, Michael R; Engelberth, Abigail S

    2016-07-08

    Acetic acid is introduced into cellulose conversion processes as a consequence of composition of lignocellulose feedstocks, causing significant inhibition of adapted, genetically modified and wild-type S. cerevisiae in bioethanol fermentation. While adaptation or modification of yeast may reduce inhibition, the most effective approach is to remove the acetic acid prior to fermentation. This work addresses liquid-liquid extraction of acetic acid from biomass hydrolysate through a pathway that mitigates acetic acid inhibition while avoiding the negative effects of the extractant, which itself may exhibit inhibition. Candidate solvents were selected using simulation results from Aspen Plus™, based on their ability to extract acetic acid which was confirmed by experimentation. All solvents showed varying degrees of toxicity toward yeast, but the relative volatility of ethyl acetate enabled its use as simple vacuum evaporation could reduce small concentrations of aqueous ethyl acetate to minimally inhibitory levels. The toxicity threshold of ethyl acetate, in the presence of acetic acid, was found to be 10 g L(-1) . The fermentation was enhanced by extracting 90% of the acetic acid using ethyl acetate, followed by vacuum evaporation to remove 88% removal of residual ethyl acetate along with 10% of the broth. NRRL Y-1546 yeast was used to demonstrate a 13% increase in concentration, 14% in ethanol specific production rate, and 11% ethanol yield. This study demonstrated that extraction of acetic acid with ethyl acetate followed by evaporative removal of ethyl acetate from the raffinate phase has potential to significantly enhance ethanol fermentation in a corn stover bioethanol facility. © 2016 American Institute of Chemical Engineers Biotechnol. Prog., 32:929-937, 2016.

  3. Hydroxide as general base in the saponification of ethyl acetate.

    PubMed

    Mata-Segreda, Julio F

    2002-03-13

    The second-order rate constant for the saponification of ethyl acetate at 30.0 degrees C in H(2)O/D(2)O mixtures of deuterium atom fraction n (a proton inventory experiment) obeys the relation k(2)(n) = 0.122 s(-1) M(-1) (1 - n + 1.2n) (1 - n + 0.48n)/(1 - n + 1.4n) (1 - n + 0.68n)(3). This result is interpreted as a process where formation of the tetrahedral intermediate is the rate-determining step and the transition-state complex is formed via nucleophilic interaction of a water molecule with general-base assistance from hydroxide ion, opposite to the direct nucleophilic collision commonly accepted. This mechanistic picture agrees with previous heavy-atom kinetic isotope effect data of Marlier on the alkaline hydrolysis of methyl formate.

  4. Stability and interface properties of thin cellulose ester films adsorbed from acetone and ethyl acetate solutions.

    PubMed

    Amim, Jorge; Kosaka, Priscila M; Petri, Denise F S; Maia, Francisco C B; Miranda, Paulo B

    2009-04-15

    Stability and interface properties of cellulose acetate propionate (CAP) and cellulose acetate butyrate (CAB) films adsorbed from acetone or ethyl acetate onto Si wafers have been investigated by means of contact angle measurements and atomic force microscopy (AFM). Surface energy (gamma(S)(total)) values determined for CAP adsorbed from acetone are larger than those from ethyl acetate. In the case of CAB films adsorbed from ethyl acetate and acetone were similar. Dewetting was observed by AFM only for CAP films prepared from ethyl acetate. Positive values of effective Hamaker constant (A(eff)) were found only for CAP prepared from ethyl acetate, corroborating with dewetting phenomena observed by AFM. On the contrary, negative values of A(eff) were determined for CAP and CAB prepared from acetone and for CAB prepared from ethyl acetate, corroborating with experimental observations. Sum frequency generation (SFG) vibrational spectra indicated that CAP and CAB films prepared from ethyl acetate present more alkyl groups oriented perpendicularly to the polymer-air interface than those films prepared from acetone. Such preferential orientation corroborates with macroscopic contact angle measurements. Moreover, SFG spectra showed that acetone binds strongly to Si wafers, creating a new surface for CAP and CAB films.

  5. Wet in situ transesterification of microalgae using ethyl acetate as a co-solvent and reactant.

    PubMed

    Park, Jeongseok; Kim, Bora; Chang, Yong Keun; Lee, Jae W

    2017-04-01

    This study addresses wet in situ transesterification of microalgae for the production of biodiesel by introducing ethyl acetate as both reactant and co-solvent. Ethyl acetate and acid catalyst are mixed with wet microalgae in one pot and the mixture is heated for simultaneous lipid extraction and transesterification. As a single reactant and co-solvent, ethyl acetate can provide higher FAEE yield and more saccharification of carbohydrates than the case of binary ethanol and chloroform as a reactant and a co-solvent. The optimal yield was 97.8wt% at 114°C and 4.06M catalyst with 6.67mlEtOAC/g dried algae based on experimental results and response surface methodology (RSM). This wet in situ transesterification of microalgae using ethyl acetate doesn't require an additional co-solvent and it also promises more economic benefit as combining extraction and transesterification in a single process.

  6. Semipurified Ethyl Acetate Partition of Methanolic Extract of Melastoma malabathricum Leaves Exerts Gastroprotective Activity Partly via Its Antioxidant-Antisecretory-Anti-Inflammatory Action and Synergistic Action of Several Flavonoid-Based Compounds

    PubMed Central

    Ismail Suhaimy, Noor Wahida; Noor Azmi, Ahmad Khusairi; Mohtarrudin, Norhafizah; Cheema, Manraj Singh

    2017-01-01

    Recent study has demonstrated the gastroprotective activity of crude methanolic extract of M. malabathricum leaves. The present study evaluated the gastroprotective potential of semipurified extracts (partitions): petroleum ether, ethyl acetate (EAMM), and aqueous obtained from the methanolic extract followed by the elucidation of the gastroprotective mechanisms of the most effective partition. Using the ethanol-induced gastric ulcer assay, all partitions exerted significant gastroprotection, with EAMM being the most effective partition. EAMM significantly (i) reduced the volume and acidity (free and total) while increasing the pH of gastric juice and enhanced the gastric wall mucus secretion when assessed using the pylorus ligation assay, (ii) increased the enzymatic and nonenzymatic antioxidant activity of the stomach tissue, (iii) lost its gastroprotective activity following pretreatment with N-omega-nitro-L-arginine methyl ester (L-NAME; NO blocker) or carbenoxolone (CBXN; NP-SH blocker), (iv) exerted antioxidant activity against various in vitro oxidation assays, and (v) showed moderate in vitro anti-inflammatory activity via the LOX-modulated pathway. In conclusion, EAMM exerts a remarkable NO/NP-SH-dependent gastroprotective effect that is attributed to its antisecretory and antioxidant activities, ability to stimulate the gastric mucus production and endogenous antioxidant system, and synergistic action of several gastroprotective-induced flavonoids. PMID:28168011

  7. Semipurified Ethyl Acetate Partition of Methanolic Extract of Melastoma malabathricum Leaves Exerts Gastroprotective Activity Partly via Its Antioxidant-Antisecretory-Anti-Inflammatory Action and Synergistic Action of Several Flavonoid-Based Compounds.

    PubMed

    Ismail Suhaimy, Noor Wahida; Noor Azmi, Ahmad Khusairi; Mohtarrudin, Norhafizah; Omar, Maizatul Hasyima; Tohid, Siti Farah Md; Cheema, Manraj Singh; Teh, Lay Kek; Salleh, Mohd Zaki; Zakaria, Zainul Amiruddin

    2017-01-01

    Recent study has demonstrated the gastroprotective activity of crude methanolic extract of M. malabathricum leaves. The present study evaluated the gastroprotective potential of semipurified extracts (partitions): petroleum ether, ethyl acetate (EAMM), and aqueous obtained from the methanolic extract followed by the elucidation of the gastroprotective mechanisms of the most effective partition. Using the ethanol-induced gastric ulcer assay, all partitions exerted significant gastroprotection, with EAMM being the most effective partition. EAMM significantly (i) reduced the volume and acidity (free and total) while increasing the pH of gastric juice and enhanced the gastric wall mucus secretion when assessed using the pylorus ligation assay, (ii) increased the enzymatic and nonenzymatic antioxidant activity of the stomach tissue, (iii) lost its gastroprotective activity following pretreatment with N-omega-nitro-L-arginine methyl ester (L-NAME; NO blocker) or carbenoxolone (CBXN; NP-SH blocker), (iv) exerted antioxidant activity against various in vitro oxidation assays, and (v) showed moderate in vitro anti-inflammatory activity via the LOX-modulated pathway. In conclusion, EAMM exerts a remarkable NO/NP-SH-dependent gastroprotective effect that is attributed to its antisecretory and antioxidant activities, ability to stimulate the gastric mucus production and endogenous antioxidant system, and synergistic action of several gastroprotective-induced flavonoids.

  8. 40 CFR 721.10074 - Acetic acid, 2-chloro-, 1-(3,3-dimethylcyclohexyl)ethyl ester.

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ...-dimethylcyclohexyl)ethyl ester. 721.10074 Section 721.10074 Protection of Environment ENVIRONMENTAL PROTECTION AGENCY... Specific Chemical Substances § 721.10074 Acetic acid, 2-chloro-, 1-(3,3-dimethylcyclohexyl)ethyl ester. (a... acetic acid, 2-chloro-, 1-(3,3-dimethylcyclohexyl)ethyl ester (PMN P-05-568; CAS No. 477218-59-0)...

  9. 40 CFR 721.10074 - Acetic acid, 2-chloro-, 1-(3,3-dimethylcyclohexyl)ethyl ester.

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ...-dimethylcyclohexyl)ethyl ester. 721.10074 Section 721.10074 Protection of Environment ENVIRONMENTAL PROTECTION AGENCY... Specific Chemical Substances § 721.10074 Acetic acid, 2-chloro-, 1-(3,3-dimethylcyclohexyl)ethyl ester. (a... acetic acid, 2-chloro-, 1-(3,3-dimethylcyclohexyl)ethyl ester (PMN P-05-568; CAS No. 477218-59-0)...

  10. 40 CFR 721.10074 - Acetic acid, 2-chloro-, 1-(3,3-dimethylcyclohexyl)ethyl ester.

    Code of Federal Regulations, 2012 CFR

    2012-07-01

    ...-dimethylcyclohexyl)ethyl ester. 721.10074 Section 721.10074 Protection of Environment ENVIRONMENTAL PROTECTION AGENCY... Specific Chemical Substances § 721.10074 Acetic acid, 2-chloro-, 1-(3,3-dimethylcyclohexyl)ethyl ester. (a... acetic acid, 2-chloro-, 1-(3,3-dimethylcyclohexyl)ethyl ester (PMN P-05-568; CAS No. 477218-59-0)...

  11. 40 CFR 721.10074 - Acetic acid, 2-chloro-, 1-(3,3-dimethylcyclohexyl)ethyl ester.

    Code of Federal Regulations, 2013 CFR

    2013-07-01

    ...-dimethylcyclohexyl)ethyl ester. 721.10074 Section 721.10074 Protection of Environment ENVIRONMENTAL PROTECTION AGENCY... Specific Chemical Substances § 721.10074 Acetic acid, 2-chloro-, 1-(3,3-dimethylcyclohexyl)ethyl ester. (a... acetic acid, 2-chloro-, 1-(3,3-dimethylcyclohexyl)ethyl ester (PMN P-05-568; CAS No. 477218-59-0)...

  12. 40 CFR 721.10074 - Acetic acid, 2-chloro-, 1-(3,3-dimethylcyclohexyl)ethyl ester.

    Code of Federal Regulations, 2014 CFR

    2014-07-01

    ...-dimethylcyclohexyl)ethyl ester. 721.10074 Section 721.10074 Protection of Environment ENVIRONMENTAL PROTECTION AGENCY... Specific Chemical Substances § 721.10074 Acetic acid, 2-chloro-, 1-(3,3-dimethylcyclohexyl)ethyl ester. (a... acetic acid, 2-chloro-, 1-(3,3-dimethylcyclohexyl)ethyl ester (PMN P-05-568; CAS No. 477218-59-0)...

  13. Ethyl Acetate Extract of Artemisia anomala S. Moore Displays Potent Anti-Inflammatory Effect.

    PubMed

    Tan, Xi; Wang, Yuan-Lai; Yang, Xiao-Lu; Zhang, Dan-Dan

    2014-01-01

    Artemisia anomala S. Moore has been widely used in China to treat inflammatory diseases for hundreds of years. However, mechanisms associated with its anti-inflammatory effect are not clear. In this study, we prepared ethyl acetate, petroleum ether, n-BuOH, and aqueous extracts from ethanol extract of Artemisia anomala S. Moore. Comparing anti-inflammatory effects of these extracts, we found that ethyl acetate extract of this herb (EAFA) exhibited the strongest inhibitory effect on nitric oxide (NO) production in LPS/IFN γ -stimulated RAW264.7 cells. EAFA suppressed the production of NO in a time- and dose-dependent manner without eliciting cytotoxicity to RAW264.7 cells. To understand the molecular mechanism underlying EAFA's anti-inflammatory effect, we showed that EAFA increased total cellular anti-oxidant capacity while reducing the amount of inducible nitric oxide synthase (iNOS) in stimulated RAW264.7 cells. EAFA also suppressed the expression of IL-1 β and IL-6, whereas it elevates the level of heme oxygenase-1. These EAFA-induced events were apparently associated with NF- κ B and MAPK signaling pathways because the DNA binding activity of p50/p65 was impaired and the activities of both ERK and JNK were decreased in EFEA-treated cells comparing to untreated cells. Our findings suggest that EAFA exerts its anti-inflammatory effect by inhibiting the expression of iNOS.

  14. Studies on the mechanism of synthesis of ethyl acetate in Kluyveromyces marxianus DSM 5422.

    PubMed

    Löser, Christian; Urit, Thanet; Keil, Peter; Bley, Thomas

    2015-02-01

    Kluyveromyces marxianus converts whey-borne sugar into ethyl acetate, an environmentally friendly solvent with many applications. K. marxianus DSM 5422 presumably synthesizes ethyl acetate from acetyl-SCoA. Iron limitation as a trigger for this synthesis is explained by a diminished aconitase and succinate dehydrogenase activity (both enzymes depend on iron) causing diversion of acetyl-SCoA from the tricarboxic acid cycle to ester synthesis. Copper limitation as another trigger for ester synthesis in this yeast refers to involvement of the electron transport chain (all ETC complexes depend on iron and complex IV requires copper). This hypothesis was checked by using several ETC inhibitors. Malonate was ineffective but carboxin partially inhibited complex II and initiated ester synthesis. Antimycin A and cyanide as complexes III and IV inhibitors initiated ester synthesis only at moderate levels while higher concentrations disrupted all respiration and caused ethanol formation. A restricted supply of oxygen (the terminal electron acceptor) also initiated some ester synthesis but primarily forced ethanol production. A switch from aerobic to anaerobic conditions nearly stopped ester synthesis and induced ethanol formation. Iron-limited ester formation was compared with anaerobic ethanol production; the ester yield was lower than the ethanol yield but a higher market price, a reduced number of process stages, a faster process, and decreased expenses for product recovery by stripping favor biotechnological ester production.

  15. Formation of ethyl acetate from whey by Kluyveromyces marxianus on a pilot scale.

    PubMed

    Löser, Christian; Urit, Thanet; Stukert, Anton; Bley, Thomas

    2013-01-10

    Whey arising in huge amounts during milk processing is a valuable renewable resource in the field of White Biotechnology. Kluyveromyces marxianus is able to convert whey-borne lactose into ethyl acetate, an environmentally friendly solvent. Formation of ethyl acetate as a bulk product is triggered by iron (Fe). K. marxianus DSM 5422 was cultivated aerobically in whey-borne medium originally containing 40 μg/L Fe, supplemented with 1, 3 or 10 mg/L Fe in the pre-culture, using an 1 L or 70 L stirred reactor. The highest Fe content in the pre-culture promoted yeast growth in the main culture causing a high sugar consumption for growth and dissatisfactory formation of ethyl acetate, while the lowest Fe content limited yeast growth and promoted ester synthesis but slowed down the process. An intermediate Fe dose (ca. 0.5 μg Fe/g sugar) lastly represented a compromise between some yeast growth, a quite high yield of ethyl acetate and an acceptable duration of the process. The mass of ethyl acetate related to the sugar consumed amounted to 0.113, 0.265 and 0.239 g/g in the three processes corresponding to 21.9%, 51.4% and 46.3% of the theoretically maximum yield. The performance on a pilot scale was somewhat higher than on lab scale.

  16. Enrichment, isolation and characterization of fungi tolerant to 1-ethyl-3-methylimidazolium acetate

    SciTech Connect

    Singer, S.W.; Reddy, A. P.; Gladden, J. M.; Guo, H.; Hazen, T.C.; Simmons, B. A.; VanderGheynst, J. S.

    2010-12-15

    This work aims to characterize microbial tolerance to 1-ethyl-3-methylimidazolium acetate ([C2mim][OAc]), ionic liquid that has emerged as a novel biomass pretreatment for lignocellulosic biomass. Enrichment experiments performed using inocula treated with [C2mim][OAc] under solid and liquid cultivation yielded fungal populationsdominated by Aspergilli. Ionic liquid-tolerant Aspergillus isolates from these enrichments were capable of growing in a radial plate growth assay in the presence of 10% [C2mim][OAc]. When a [C2mim][OAc]-tolerant Aspergillus fumigatus strain was grown in the presence of switchgrass, endoglucanases and xylanases were secreted that retained residual enzymatic activity in the presence of 20% [C2mim][OAc]. The results of the study suggest tolerance to ionic liquids is a general property of Aspergilli. Tolerance to an industrially important ionic liquid was discovered in a fungal genera that is widely used in biotechnology, including biomass deconstruction.

  17. Two new cucurbitane-type triterpenoid saponins isolated from ethyl acetate extract of Citrullus colocynthis fruit.

    PubMed

    Song, Fei; Dai, Bin; Zhang, Hai-Yan; Xie, Jian-Wei; Gu, Cheng-Zhi; Zhang, Jie

    2015-01-01

    Two new cucurbitacins I (1 and 2), together with eight known compounds (3-10), were isolated from the ethyl acetate extract of the fruit of Citrullus colocynthis. Compounds 3, 5-9 were isolated from C. colocynthis for the first time. The structures of new compounds were determined primarily from IR, HR-MS, 1D-, and 2D-NMR analysis.

  18. Experimental Determination of Densities and Isobaric Vapor-Liquid Equilibria of Methyl Acetate and Ethyl Acetate with Alcohols (C3 and C4) at 0.3 MPa

    NASA Astrophysics Data System (ADS)

    Susial, Pedro; Estupiñan, Esteban J.; Castillo, Victor D.; Rodríguez-Henríquez, José J.; Apolinario, José C.

    2013-10-01

    The densities and excess volumes were determined at 298.15 K for the methyl acetate + 1-propanol, methyl acetate + 1-butanol, and ethyl acetate + 1-butanol mixtures. The vapor-liquid equilibria data at 0.3 MPa for these binary systems were obtained using a stainless steel equilibrium still. The activity coefficients were obtained from the experimental data using the Hayden and O’Connell method and the Yen and Woods equation. The binary systems in this study showed positive deviations from ideality. The experimental VLE data were verified with the point-to-point test of van Ness using the Barker routine and the Fredenslund criterion. The different versions of the UNIFAC and the ASOG group contribution models were applied.

  19. Crystal structures of the solvates of diethylaminogossypol with ethyl acetate and pyridine

    Technology Transfer Automated Retrieval System (TEKTRAN)

    The crystal structures of diethylaminogossypol with ethyl acetate (DEAG-EA) and pyridine (DEAG-P) were studied by room-temperature X-ray diffraction. The host-to-guest molecule ratio in these complexes is 2:1 for DEAG-EA and 2:5 for DEAG-P. The crystal and cell parameters for DEAG-EA are C34H40N2O6...

  20. Location and Mapping of an Ethyl Acetate Plume in Mexico City

    NASA Astrophysics Data System (ADS)

    Rogers, T.; Grimsrud, E.; Knighton, W.; Velasco, E.; Lamb, B.; Westberg, H.; Jobson, T.; Alexander, M.; Prazeller, P.; Herndon, S.; Kolb, C.

    2004-12-01

    A major goal of the 2003 Mexico City Metropolitan Area (MCMA) field campaign was to gain a better understanding of the dispersion and transport of volatile organic compounds (VOCs) in this urban airshed. Continuous monitoring of VOCs in the atmosphere and identification and quantification of their emission sources is complicated by two factors: first, there are hundreds of different VOC species released daily in the MCMA atmosphere, and second, few real time (1-10 second) measurement techniques have been available to provide the high resolution spatial and/or temporal data usually required to locate VOC emission sources and measure their flux strength. A relatively new technique, Proton Transfer Reaction Mass Spectometery (PTR-MS) provides this capability and was used to locate and quantify a significant source of ethyl acetate in the Iztapalapa region of Mexico City. Two PTR-MS systems were deployed during the 2003 MCMA campaign, the MSU PTR-MS was operated on-board the Aerodyne Mobile Laboratory while the PNNL instrument located on the roof at the National Center for Environmental Research and Training (Centro Nacional de Investigacion y Capacitacion Ambiental or CENICA). The uniqueness of the ethyl acetate signature allowed the MSU PTR-MS on-board the mobile lab to track the ethyl acetate plume back to its source. A short movie documenting the plume mapping and location of the source of the ethyl acetate emission will be shown. Knowing of the plume source location and the local meteorological conditions, the time resolved responses from the PNNL PTR-MS at the CENCIA location have been applied to a simple plume model to estimate the plume's emission flux strength.

  1. Detoxification of biomass derived acetate via metabolic conversion to ethanol, acetone, isopropanol, or ethyl acetate

    DOEpatents

    Sillers, William Ryan; Van Dijken, Hans; Licht, Steve; Shaw, IV, Arthur J.; Gilbert, Alan Benjamin; Argyros, Aaron; Froehlich, Allan C.; McBride, John E.; Xu, Haowen; Hogsett, David A.; Rajgarhia, Vineet B.

    2017-03-28

    One aspect of the invention relates to a genetically modified thermophilic or mesophilic microorganism, wherein a first native gene is partially, substantially, or completely deleted, silenced, inactivated, or down-regulated, which first native gene encodes a first native enzyme involved in the metabolic production of an organic acid or a salt thereof, thereby increasing the native ability of said thermophilic or mesophilic microorganism to produce lactate or acetate as a fermentation product. In certain embodiments, the aforementioned microorganism further comprises a first non-native gene, which first non-native gene encodes a first non-native enzyme involved in the metabolic production of lactate or acetate. Another aspect of the invention relates to a process for converting lignocellulosic biomass to lactate or acetate, comprising contacting lignocellulosic biomass with a genetically modified thermophilic or mesophilic microorganism.

  2. Use of a Batch Reactive Distillation with Dynamic Optimization Strategy to Achieve Industrial Grade Ethyl Acetate

    NASA Astrophysics Data System (ADS)

    Konakom, Kwantip; Saengchan, Aritsara; Kittisupakorn, Paisan; Mujtaba, Iqbal M.

    2011-08-01

    Industrial grade ethyl acetate is available with minimum purity of 85.0%. It is mostly produced by an ethanol esterification in a distillation process on both batch and continuous modes. However, researches on high purity production with short operating time are rarely achieved. Therefore, the objective in this work is to study an approach to produce ethyl acetate of 90.0% by 8 hours using a batch reactive distillation column. Based on open-loop simulations, the distillation with constant reflux ratio cannot achieve the product specification. Thus, the dynamic optimization strategy is proposed to handle this problem. For the process safety—preventing the dried column and fractured, a minimum reflux ratio must be determined in advance and then an optimal reflux profile is calculated to achieve optimal product yield. Simulation results show that the industrial grade ethyl acetate can be produced by the dynamic optimization programming with two or more time intervals. Besides, the increasing of time intervals can produce more distillate product.

  3. Synthesis of Highly Polymerized Water-soluble Cellulose Acetate by the Side Reaction in Carboxylate Ionic Liquid 1-ethyl-3-methylimidazolium Acetate.

    PubMed

    Pang, Jinhui; Liu, Xin; Yang, Jun; Lu, Fachuang; Wang, Bo; Xu, Feng; Ma, Mingguo; Zhang, Xueming

    2016-09-20

    In the present study, we describe a novel one-step method to prepare water-soluble cellulose acetate (WSCA) with higher degree of polymerization values (DP = 650-680) by in situ activation of carboxyl group in ionic liquid. First of all, cellulose was dissolved in 1-ethyl-3-methylimidazolium acetate (EmimAc) and reacted with dichloroacetyl chloride (Cl2AcCl) in order to make cellulose dichloroacetate. Under various conditions, a series of water soluble products were produced. Elemental analysis and NMR results confirmed that they were cellulose acetate with DS (degree of substitution) values in the range from 0.30 to 0.63. NMR studies demonstrated that Cl2AcCl reacted with acetate anion of EmimAc producing a mixed anhydride that acetylated cellulose. Other acylating reagents such as benzoyl chloride, chloroacetyl chloride can also work similarly. 2D NMR characterization suggested that 6-mono-O-acetyl moiety, 3,6-di-O-acetylcellulose and 2,6-di-O-acetyl cellulose were all synthesized and the reactivity of hydroxyl groups in anhydro-glucose units was in the order C-6>C-3>C-2. This work provides an alternative way to make WSCA, meanwhile, also services as a reminder that the activity of EmimAc toward carbohydrate as acylating reagents could be a problem, because the expected acylated products may not be resulted and recycling of this ionic liquid could also be difficult.

  4. Synthesis of Highly Polymerized Water-soluble Cellulose Acetate by the Side Reaction in Carboxylate Ionic Liquid 1-ethyl-3-methylimidazolium Acetate

    NASA Astrophysics Data System (ADS)

    Pang, Jinhui; Liu, Xin; Yang, Jun; Lu, Fachuang; Wang, Bo; Xu, Feng; Ma, Mingguo; Zhang, Xueming

    2016-09-01

    In the present study, we describe a novel one-step method to prepare water-soluble cellulose acetate (WSCA) with higher degree of polymerization values (DP = 650–680) by in situ activation of carboxyl group in ionic liquid. First of all, cellulose was dissolved in 1-ethyl-3-methylimidazolium acetate (EmimAc) and reacted with dichloroacetyl chloride (Cl2AcCl) in order to make cellulose dichloroacetate. Under various conditions, a series of water soluble products were produced. Elemental analysis and NMR results confirmed that they were cellulose acetate with DS (degree of substitution) values in the range from 0.30 to 0.63. NMR studies demonstrated that Cl2AcCl reacted with acetate anion of EmimAc producing a mixed anhydride that acetylated cellulose. Other acylating reagents such as benzoyl chloride, chloroacetyl chloride can also work similarly. 2D NMR characterization suggested that 6-mono-O-acetyl moiety, 3,6-di-O-acetylcellulose and 2,6-di-O-acetyl cellulose were all synthesized and the reactivity of hydroxyl groups in anhydro-glucose units was in the order C-6>C-3>C-2. This work provides an alternative way to make WSCA, meanwhile, also services as a reminder that the activity of EmimAc toward carbohydrate as acylating reagents could be a problem, because the expected acylated products may not be resulted and recycling of this ionic liquid could also be difficult.

  5. Synthesis of Highly Polymerized Water-soluble Cellulose Acetate by the Side Reaction in Carboxylate Ionic Liquid 1-ethyl-3-methylimidazolium Acetate

    PubMed Central

    Pang, Jinhui; Liu, Xin; Yang, Jun; Lu, Fachuang; Wang, Bo; Xu, Feng; Ma, Mingguo; Zhang, Xueming

    2016-01-01

    In the present study, we describe a novel one-step method to prepare water-soluble cellulose acetate (WSCA) with higher degree of polymerization values (DP = 650–680) by in situ activation of carboxyl group in ionic liquid. First of all, cellulose was dissolved in 1-ethyl-3-methylimidazolium acetate (EmimAc) and reacted with dichloroacetyl chloride (Cl2AcCl) in order to make cellulose dichloroacetate. Under various conditions, a series of water soluble products were produced. Elemental analysis and NMR results confirmed that they were cellulose acetate with DS (degree of substitution) values in the range from 0.30 to 0.63. NMR studies demonstrated that Cl2AcCl reacted with acetate anion of EmimAc producing a mixed anhydride that acetylated cellulose. Other acylating reagents such as benzoyl chloride, chloroacetyl chloride can also work similarly. 2D NMR characterization suggested that 6-mono-O-acetyl moiety, 3,6-di-O-acetylcellulose and 2,6-di-O-acetyl cellulose were all synthesized and the reactivity of hydroxyl groups in anhydro-glucose units was in the order C-6>C-3>C-2. This work provides an alternative way to make WSCA, meanwhile, also services as a reminder that the activity of EmimAc toward carbohydrate as acylating reagents could be a problem, because the expected acylated products may not be resulted and recycling of this ionic liquid could also be difficult. PMID:27644545

  6. Electrochemical Partial Reforming of Ethanol into Ethyl Acetate Using Ultrathin Co3O4 Nanosheets as a Highly Selective Anode Catalyst

    PubMed Central

    2016-01-01

    Electrochemical partial reforming of organics provides an alternative strategy to produce valuable organic compounds while generating H2 under mild conditions. In this work, highly selective electrochemical reforming of ethanol into ethyl acetate is successfully achieved by using ultrathin Co3O4 nanosheets with exposed (111) facets as an anode catalyst. Those nanosheets were synthesized by a one-pot, templateless hydrothermal method with the use of ammonia. NH3 was demonstrated critical to the overall formation of ultrathin Co3O4 nanosheets. With abundant active sites on Co3O4 (111), the as-synthesized ultrathin Co3O4 nanosheets exhibited enhanced electrocatalytic activities toward water and ethanol oxidations in alkaline media. More importantly, over the Co3O4 nanosheets, the electrooxidation from ethanol to ethyl acetate was so selective that no other oxidation products were yielded. With such a high selectivity, an electrolyzer cell using Co3O4 nanosheets as the anode electrocatalyst and Ni–Mo nanopowders as the cathode electrocatalyst has been successfully built for ethanol reforming. The electrolyzer cell was readily driven by a 1.5 V battery to achieve the effective production of both H2 and ethyl acetate. After the bulk electrolysis, about 95% of ethanol was electrochemically reformed into ethyl acetate. This work opens up new opportunities in designing a material system for building unique devices to generate both hydrogen and high-value organics at room temperature by utilizing electric energy from renewable sources. PMID:27610415

  7. The antihypertensive effect of ethyl acetate extract of radish leaves in spontaneously hypertensive rats

    PubMed Central

    Chung, Da-Hee; Kim, Sun-Hee; Myung, Nahye; Cho, Kang Jin

    2012-01-01

    Radish (Raphanus sativus L.) is a cruciferous vegetable, and its leaves have antioxidant and anticancer properties. This study was conducted to evaluate the effects of ethyl acetate extracts from radish leaves on hypertension in 11-week-old spontaneously hypertensive rats (SHRs). The SHRs were randomly divided into 3 groups of 6 rats each on the basis of initial systolic blood pressure (SBP) and were treated with oral administration of radish leaf extract (0, 30, or 90 mg/kg body weight [bw], respectively) for 5 weeks. Six Wistar rats were used as normotensive controls. The amount of the radish leaf extract had no effect on body weight. The SBP of the SHRs showed a decreasing trend with the consumption of the radish leaf extract. In the third week, the SBP of the group fed 90 mg extract/kg bw reduced from 214 mmHg to 166 mmHg and was significantly lower than that of the normotensive and hypertensive controls. The extract did not show a significant effect on the angiotensin-converting enzyme (ACE) activity in the serum, kidney, and lung. The extract increased the concentration of NO in serum and the activities of antioxidant enzymes such as glutathione peroxidase and catalase in red blood cells (RBCs). The serum concentrations of Na+ and K+ were not significantly different between all groups. However, the fecal concentrations of Na+ and K+ increased; the fecal concentrations of Na+ and K+ for the normotensive and hypertensive controls were not different. Urinary excretion of Na+ was higher in the normotensive Wistar rats than in the SHRs, while that of K+ was not significantly different. These findings indicate that consumption of radish leaves might have had antihypertensive effects in SHRs by increasing the serum concentration of NO and fecal concentration of Na+ and enhancing antioxidant activities. PMID:22977684

  8. Effects of ethyl acetate extract of Kaempferia parviflora on brown adipose tissue.

    PubMed

    Kobayashi, Hiroko; Horiguchi-Babamoto, Emi; Suzuki, Mio; Makihara, Hiroko; Tomozawa, Hiroshi; Tsubata, Masahito; Shimada, Tsutomu; Sugiyama, Kiyoshi; Aburada, Masaki

    2016-01-01

    We have previously reported the effects of Kaempferia parviflora (KP), including anti-obesity, preventing various metabolic diseases, and regulating differentiation of white adipose cells. In this study we used Tsumura, Suzuki, Obese Diabetes (TSOD) mice--an animal model of spontaneous obese type II diabetes--and primary brown preadipocytes to examine the effects of the ethyl acetate extract of KP (KPE) on brown adipose tissue, which is one of the energy expenditure organs. TSOD mice were fed with MF mixed with either KPE 0.3 or 1% for 8 weeks. Computed tomography images showed that whitening of brown adipocytes was suppressed in the interscapular tissue of the KPE group. We also examined mRNA expression of uncoupling protein 1 (UCP-1) and β3-adrenalin receptor (β3AR) in brown adipose tissue. As a result, mRNA expression of UCP-1 significantly increased in the KPE 1% treatment group, indicating that KPE activated brown adipose tissue. We then evaluated the direct effects of KPE on brown adipocytes using primary brown preadipocytes isolated from interscapular brown adipocytes in ICR mice. Triacylglycerol (TG) accumulation in primary brown preadipocytes was increased by KPE in a dose-dependent manner. Each mRNA expression of peroxisome proliferator-activated receptor γ (PPARγ), UCP-1, and β3AR exhibited an upward trend compared with the control group. Moreover, some polymethoxyflavonoids (PMFs), the main compound in KP, also increased TG accumulation. This study therefore showed that KPE enhanced the thermogenesis effect of brown adipocytes as well as promoted the differentiation of brown adipocyte cells.

  9. Ethyl 2-(2-methyl-1H-benzimidazol-1-yl)acetate

    PubMed Central

    Xu, Guang-Hai; Wang, Wei

    2008-01-01

    A new benzimidazole compound, C12H14N2O2, has been synthesized by the reaction of 2-methyl-1H-benzimidazole and ethyl 2-bromo­acetate. In the crystal structure, weak inter­molecular C—H⋯N hydrogen bonds link the mol­ecules into chains. π⋯π Contacts (centroid⋯centroid distance = 3.713 Å) are observed. A C—H⋯π inter­action is also present. The N—C—C—O torsion angle is 178.4 (2)°. PMID:21201788

  10. Rapid detergent removal from peptide samples with ethyl acetate for mass spectrometry analysis.

    PubMed

    Yeung, Yee-Guide; Stanley, E Richard

    2010-02-01

    Detergents are required for the extraction of hydrophobic proteins and for the maintenance of their solubility in solution. However, the presence of detergents in the peptide samples severely suppresses ionization in mass spectrometry (MS) analysis and decreases chromatographic resolution in LC-MS. Thus, detergents must be removed for sensitive detection of peptides by MS. This unit describes a rapid protocol in which ethyl acetate extraction is used to remove octylglucoside from protease digests without loss of peptides. This procedure can also be used to reduce interference by sodium dodecyl sulfate, Nonidet P-40, or Triton X-100 in peptide samples for MS analysis.

  11. Understanding the hydrolysis mechanism of ethyl acetate catalyzed by an aqueous molybdocene: a computational chemistry investigation.

    PubMed

    Tílvez, Elkin; Cárdenas-Jirón, Gloria I; Menéndez, María I; López, Ramón

    2015-02-16

    A thoroughly mechanistic investigation on the [Cp2Mo(OH)(OH2)](+)-catalyzed hydrolysis of ethyl acetate has been performed using density functional theory methodology together with continuum and discrete-continuum solvation models. The use of explicit water molecules in the PCM-B3LYP/aug-cc-pVTZ (aug-cc-pVTZ-PP for Mo)//PCM-B3LYP/aug-cc-pVDZ (aug-cc-pVDZ-PP for Mo) computations is crucial to show that the intramolecular hydroxo ligand attack is the preferred mechanism in agreement with experimental suggestions. Besides, the most stable intermediate located along this mechanism is analogous to that experimentally reported for the norbornenyl acetate hydrolysis catalyzed by molybdocenes. The three most relevant steps are the formation and cleavage of the tetrahedral intermediate immediately formed after the hydroxo ligand attack and the acetic acid formation, with the second one being the rate-determining step with a Gibbs energy barrier of 36.7 kcal/mol. Among several functionals checked, B3LYP-D3 and M06 give the best agreement with experiment as the rate-determining Gibbs energy barrier obtained only differs 0.2 and 0.7 kcal/mol, respectively, from that derived from the experimental kinetic constant measured at 296.15 K. In both cases, the acetic acid elimination becomes now the rate-determining step of the overall process as it is 0.4 kcal/mol less stable than the tetrahedral intermediate cleavage. Apart from clarifying the identity of the cyclic intermediate and discarding the tetrahedral intermediate formation as the rate-determining step for the mechanism of the acetyl acetate hydrolysis catalyzed by molybdocenes, the small difference in the Gibbs energy barrier found between the acetic acid formation and the tetrahedral intermediate cleavage also uncovers that the rate-determining step could change when studying the reactivity of carboxylic esters other than ethyl acetate substrate specific toward molybdocenes or other transition metal complexes. Therefore

  12. Isolation of ethyl acetic based AGF bio-nutrient and its application on the growth of Capsicum annum L. plants

    NASA Astrophysics Data System (ADS)

    Hendrawan, Sonjaya, Yaya; Khoerunnisa, Fitri; Musthapa, Iqbal; Nurmala, Astri Rizki

    2015-12-01

    The study aimed to obtain the bionutrient derived from extraction of AGF leafs in ethyl acetic solvents and to explore its application on the plant growth of capsicum annum L. (curly red chili). Particularly, the fraction of secondary metabolites groups composed bionutrient was intensively elucidated by liquid vacuum chromatography technique. The characterization of secondary metabolites groups was conducted through several methods, i.e. thin layer chromatography, phytochemical screening, and FTIR spectroscopy. The AGF extracts based bionutrient then was applied on capsicum annum L. plants with dosage of 2 and 10 mL/L. The ethyl acetic solvent and commercial nutrient of Phonska and pesticide of curacron (EC 500) were selected as a blank and a positive control to evaluate the growth pattern of capsicum annum L., respectively. The result showed that the CF 1 dan CF2 of AGF extract contained alkaloid and terpenoid of secondary metabolite group, the CF 3, and CF 4 of AGF extracts were dominated by alkaloid, flavonoid, and terpenoid, while the CF 5 of AGF extract contained alkaloid, tannin and terpenoid groups. The CF 2 of AGF extract has the highest growth rate constant of 0.1702 week-1 with the number and heaviest mass of the yield of 82 pieces and 186.60, respectively. It was also showed the significant bio-pesticide activity that should be useful to support plant growth, indicating that AGF extract can be applied as both bio-nutrient and bio-pesticide.

  13. Formation of ethyl acetate by Kluyveromyces marxianus on whey during aerobic batch cultivation at specific trace element limitation.

    PubMed

    Urit, Thanet; Stukert, Anton; Bley, Thomas; Löser, Christian

    2012-12-01

    Kluyveromyces marxianus is able to transform lactose into ethyl acetate as a bulk product which offers a chance for an economical reuse of whey-borne sugar. Ethyl acetate is highly volatile and allows its process-integrated recovery by stripping from the aerated bioreactor. Extensive formation of ethyl acetate by K. marxianus DSM 5422 required restriction of yeast growth by a lack of trace elements. Several aerobic batch processes were done in a 1-L stirred reactor using whey-borne culture medium supplemented with an individual trace element solution excluding Mn, Mo, Fe, Cu, or Zn for identifying the trace element(s) crucial for the observed ester synthesis. Only a lack of Fe, Cu, or Zn restricted yeast growth while exclusion of Mn and Mo did not exhibit any effect due to a higher amount of the latter in the used whey. Limitation of growth by Fe or Cu caused significant production of ethyl acetate while limitation by Zn resulted in formation of ethanol. A lack of Fe or Cu obviously makes the respiratory chain inefficient resulting in an increased mitochondrial NADH level followed by a reduced metabolic flux of acetyl-SCoA into the citrate cycle. Synthesis of ethyl acetate from acetyl-SCoA and ethanol by alcoholysis is thus interpreted as an overflow metabolism.

  14. Nanofiltration of rhodium tris(triphenylphosphine) catalyst in ethyl acetate solution

    NASA Astrophysics Data System (ADS)

    Shaharun, Maizatul S.; Mustafa, Ahmad K.; Taha, Mohd F.

    2012-09-01

    Solvent resistant nanofiltration (SRNF) using polymer membranes has recently received enhanced attention due to the search for cleaner and more energy-efficient technologies. The large size of the rhodium tris(triphenylphosphine) [HRh(CO)(PPh3)3] catalyst (>400 Da) - relative to other components of the hydroformylation reaction provides the opportunity for a membrane separation based on retention of the catalyst species while permeating the solvent. The compatibility of the solvent-polyimide membrane (DuraMem{trade mark, serif} 200 and DuraMem{trade mark, serif} 500) combinations was assessed in terms of the membrane stability in solvent plus non-zero solvent flux at 2.0 MPa. Good HRh(CO)(PPh3)3 rejection (>0.95) and solvent fluxes of 9.9 L/m2ṡh1 at 2.0 MPa were obtained in the catalyst-ethyl acetate-DuraMem 500 system. The effect of pressure and catalyst concentration on the solvent flux and catalyst rejection was conducted on the catalyst-ethyl acetate-membrane systems. Increasing pressure substantially improved both solvent flux and catalyst rejection, while increasing catalyst concentration was found to be beneficial in terms of substantial increases in catalyst rejection without significantly affecting solvent flux.

  15. Hormetic effect of ionic liquid 1-ethyl-3-methylimidazolium acetate on bacteria

    SciTech Connect

    Nancharaiah, Y. V.; Francis, A. J.

    2015-02-19

    The biological effect of ionic liquids (ILs) is one of the highly debated topics as they are being contemplated for various industrial applications. 1-ethyl-2-methylimidazolium acetate ([EMIM][Ac]) showed remarkable hormesis on anaerobic Clostridium sp. and aerobic Psueudomonas putida. Bacterial growth was stimulated at up to 2.5 g L-1 and inhibited at > 2.5 g L-1 of ([EMIM][Ac]). The growth of Clostridium sp. and P. putida were higher by 0.4 and 4-fold respectively, in the presense of 0.5 g L-1 of ([EMIM][Ac]). Assessment of the effect of [EMIM][Ac] under different growth conditions showed that the hormesis of [EMIM][Ac] was mediated via regulation of medium pH. Hormetic effect of [EMIM][Ac] was evident only in medium with poor buffering capacity and in the presence of a fermentable substrate as the carbon source. The hormetic effect of [EMIM][Ac] on bacterial growth is most likely associated with the buffering capacity of acetate anion. These observations have implications in ILs toxicity studies and ecological risk assessment.

  16. Hormetic effect of ionic liquid 1-ethyl-3-methylimidazolium acetate on bacteria

    DOE PAGES

    Nancharaiah, Y. V.; Francis, A. J.

    2015-02-19

    The biological effect of ionic liquids (ILs) is one of the highly debated topics as they are being contemplated for various industrial applications. 1-ethyl-2-methylimidazolium acetate ([EMIM][Ac]) showed remarkable hormesis on anaerobic Clostridium sp. and aerobic Psueudomonas putida. Bacterial growth was stimulated at up to 2.5 g L-1 and inhibited at > 2.5 g L-1 of ([EMIM][Ac]). The growth of Clostridium sp. and P. putida were higher by 0.4 and 4-fold respectively, in the presense of 0.5 g L-1 of ([EMIM][Ac]). Assessment of the effect of [EMIM][Ac] under different growth conditions showed that the hormesis of [EMIM][Ac] was mediated via regulationmore » of medium pH. Hormetic effect of [EMIM][Ac] was evident only in medium with poor buffering capacity and in the presence of a fermentable substrate as the carbon source. The hormetic effect of [EMIM][Ac] on bacterial growth is most likely associated with the buffering capacity of acetate anion. These observations have implications in ILs toxicity studies and ecological risk assessment.« less

  17. Validation of an Efficient Method for the Determination of Pesticide Residues in Fruits and Vegetables Using Ethyl Acetate for Extraction

    Technology Transfer Automated Retrieval System (TEKTRAN)

    In this study, a version of the “quick, easy, cheap, effective, rugged, and safe” (QuEChERS) method was modified to use ethyl acetate (EtOAc) rather than acetonitrile (MeCN) for extraction in the determination of multiple pesticide residues in fruits and vegetables. EtOAc is better suited than MeCN...

  18. In-vivo Antioxidant Effects of Ethyl Acetate Fraction of Mentha spicata L. on 4-Nitroquinoline-1-Oxide Injected Mice.

    PubMed

    Arumugam, Ponnan; Ramesh, Arabandi

    2011-01-01

    Antioxidant effects of ethyl acetate fraction of Mentha spicata (L.) were evaluated against 4-nitroquinoline-1-oxide injected mice. For this study, experiment setup consisted of 36 albino mice of either sex divided into 6 groups: Control (25% DMSO in water), ethyl acetate fraction (EAF) alone group (80, 160 mg/Kg body weight-bwt), 4-NQO (7.5 mg/Kg bwt-IP) alone and 4-NQO + EAF. EAF and vehicles were administered orally for five consecutive days. 4-NQO (7.5 mg/Kg bwt) was injected intraperitoneally on the 6(th) day. After 24 h, the animals were killed; liver sample was extracted and used for bio-assay. 4-NQO alone treated group decreased (27-60%) the antioxidant activities and promoted lipid peroxidation (LPO-60%) over their respective control values. Pretreatment with EAF, at the maximum dose (160 mg/Kg bwt) brought down the LPO up to 87% enhanced by 4-NQO. Among the enzymatic antioxidants, glutathione S-transferase (GST) was the most affected enzyme with 4-NQO and the least was catalase (CAT). Pretreatment with EAF (160 mg/Kg bwt), the restoration of antioxidants like glutathione peroxidase, superoxide dismutase, and CAT were found equal or less than 1.2 fold higher than that of the respective control values whereas, GST was observed to be the most restored antioxidant. Be reduced glutathione (GSH) and the least vitamin C over their control values. EAF restored the GSH and Vitamin E levels were found to be 1.2 fold higher than the respective control values.

  19. Potential biofuel additive from renewable sources--Kinetic study of formation of butyl acetate by heterogeneously catalyzed transesterification of ethyl acetate with butanol.

    PubMed

    Ali, Sami H; Al-Rashed, Osama; Azeez, Fadhel A; Merchant, Sabiha Q

    2011-11-01

    Butyl acetate holds great potential as a sustainable biofuel additive. Heterogeneously catalyzed transesterification of biobutanol and bioethylacetate can produce butyl acetate. This route is eco-friendly and offers several advantages over the commonly used Fischer Esterification. The Amberlite IR 120- and Amberlyst 15-catalyzed transesterification is studied in a batch reactor over a range of catalyst loading (6-12 wt.%), alcohol to ester feed ratio (1:3 to 3:1), and temperature (303.15-333.15K). A butanol mole fraction of 0.2 in the feed is found to be optimum. Amberlite IR 120 promotes faster kinetics under these conditions. The transesterifications studied are slightly exothermic. The moles of solvent sorbed per gram of catalyst decreases (ethanol>butanol>ethyl acetate>butyl acetate) with decrease in solubility parameter. The dual site models, the Langmuir Hinshelwood and Popken models, are the most successful in correlating the kinetics over Amberlite IR 120 and Amberlyst 15, respectively.

  20. Identification of Neuroactive Constituents of the Ethyl Acetate Fraction from Cyperi Rhizoma Using Bioactivity-Guided Fractionation

    PubMed Central

    Sim, Yeomoon; Choi, Jin Gyu; Gu, Pil Sung; Ryu, Byeol; Kim, Jeong Hee; Kang, Insug; Jang, Dae Sik; Oh, Myung Sook

    2016-01-01

    Cyperi Rhizoma (CR), the rhizome of Cyperus rotundus L., exhibits neuroprotective effects in in vitro and in vivo models of neuronal diseases. Nevertheless, no study has aimed at finding the neuroactive constituent(s) of CR. In this study, we identified active compounds in a CR extract (CRE) using bioactivity-guided fractionation. We first compared the anti-oxidative and neuroprotective activities of four fractions and the CRE total extract. Only the ethyl acetate (EA) fraction revealed strong activity, and further isolation from the bioactive EA fraction yielded nine constituents: scirpusin A (1), scirpusin B (2), luteolin (3), 6′-acetyl-3,6-diferuloylsucrose (4), 4′,6′ diacetyl-3,6-diferuloylsucrose (5), p-coumaric acid (6), ferulic acid (7), pinellic acid (8), and fulgidic acid (9). The activities of constituents 1–9 were assessed in terms of anti-oxidative, neuroprotective, anti-inflammatory, and anti-amyloid-β activities. Constituents 1, 2, and 3 exhibited strong activities; constituents 1 and 2 were characterized for the first time in this study. These results provide evidence for the value of CRE as a source of multi-functional neuroprotectants, and constituents 1 and 2 may represent new candidates for further development in therapeutic use against neurodegenerative diseases. PMID:27350341

  1. Vesicles protect activated acetic acid.

    PubMed

    Todd, Zoe R; House, Christopher H

    2014-10-01

    Abstract Methyl thioacetate, or activated acetic acid, has been proposed to be central to the origin of life and an important energy currency molecule in early cellular evolution. We have investigated the hydrolysis of methyl thioacetate under various conditions. Its uncatalyzed rate of hydrolysis is about 3 orders of magnitude faster (K=0.00663 s(-1); 100°C, pH 7.5, concentration=0.33 mM) than published rates for its catalyzed production, making it unlikely to accumulate under prebiotic conditions. However, our experiments showed that methyl thioacetate was protected from hydrolysis when inside its own hydrophobic droplets. Further, we found that methyl thioacetate protection from hydrolysis was also possible in droplets of hexane and in the membranes of nonanoic acid vesicles. Thus, the hydrophobic regions of prebiotic vesicles and early cell membranes could have offered a refuge for this energetic molecule, increasing its lifetime in close proximity to the reactions for which it would be needed. This model of early energy storage evokes an additional critical function for the earliest cell membranes.

  2. Physical insight into switchgrass dissolution in the ionic liquid 1-ethyl-3-methylimidazolium acetate

    SciTech Connect

    Wang, Hui; Gurau, Gabriela; Pingali, Sai Venkatesh; O'Neil, Hugh; Evans, Barbara R; Urban, Volker S; Heller, William T; Rogers, Robin D

    2014-01-01

    Small-angle neutron scattering was used to characterize solutions of switchgrass and the constituent biopolymers cellulose, hemicellulose, and lignin, as well as a physical mixture of them mimicking the composition of switchgrass, dissolved in the ionic liquid (IL) 1-ethyl-3-methylimidazolium acetate. The results demonstrate that the IL dissolves the cellulose fibrils of switchgrass, although a supramolecular biopolymer network remains that is not present in solutions of the individual biopolymers and that does not self-assemble in a solution containing the physical mixture of the individual biopolymers. The persistence of a network-like structure indicates that dissolving switchgrass in the IL does not disrupt all of the physical entanglements and covalent linkages between the biopolymers created during plant growth. Reconstitution of the IL-dissolved switchgrass yields carbohydrate-rich material containing cellulose with a low degree of crystallinity, as determined by powder X-ray diffraction, which impacts potential down-stream uses of the biopolymers produced by the process. The data suggests that the use of chemical additives which would break bonds that exist between the lignin and hemicellulose might improve the purity of the resulting product, but may not be able to disrupt the highly physically-entangled biopolymer network sufficiently to facilitate their separation.

  3. Impact of ionic liquid pretreatment conditions on cellulose crystalline structure using 1-ethyl-3-methylimidazolium acetate.

    PubMed

    Cheng, Gang; Varanasi, Patanjali; Arora, Rohit; Stavila, Vitalie; Simmons, Blake A; Kent, Michael S; Singh, Seema

    2012-08-23

    Ionic liquids (ILs) have been shown to affect cellulose crystalline structure in lignocellulosic biomass during pretreatment. A systematic investigation of the swelling and dissolution processes associated with IL pretreatment is needed to better understand cellulose structural transformation. In this work, 3-20 wt % microcrystalline cellulose (Avicel) solutions were treated with 1-ethyl-3-methylimidazolium acetate ([C(2)mim][OAc]) and a mixture of [C(2)mim][OAc] with the nonsolvent dimethyl sulfoxide (DMSO) at different temperatures. The dissolution process was slowed by decreasing the temperature and increasing cellulose loading, and was further retarded by addition of DMSO, enabling in-depth examination of the intermediate stages of dissolution. Results show that the cellulose I lattice expands and distorts prior to full dissolution in [C(2)mim][OAc] and that upon precipitation the former structure leads to a less ordered intermediate structure, whereas fully dissolved cellulose leads to a mixture of cellulose II and amorphous cellulose. Enzymatic hydrolysis was more rapid for the intermediate structure (crystallinity = 0.34) than for cellulose II (crystallinity = 0.54).

  4. PCL-gelatin composite nanofibers electrospun using diluted acetic acid-ethyl acetate solvent system for stem cell-based bone tissue engineering.

    PubMed

    Binulal, N S; Natarajan, Amrita; Menon, Deepthy; Bhaskaran, V K; Mony, Ullas; Nair, Shantikumar V

    2014-01-01

    Composite nanofibrous scaffolds with various poly(ε-caprolactone) (PCL)/gelatin ratios (90:10, 80:20, 70:30, 60:40, 50:50 wt.%) were successfully electrospun using diluted acetic and ethyl acetate mixture. The effects of this solvent system on the solution properties of the composites and its electrospinning properties were investigated. Viscosity and conductivity of the solutions, with the addition of gelatin, allowed for the electrospinning of uniform nanofibers with increasing hydrophilicity and degradation. Composite nanofibers containing 30 and 40 wt.% gelatin showed an optimum combination of hydrophilicity and degradability and also maintained the structural integrity of the scaffold. Human mesenchymal stem cells (hMSCs) showed favorable interaction with and proliferation on, the composite scaffolds. hMSC proliferation was highest in the 30 and 40 wt.% gelatin containing composites. Our experimental data suggested that PCL-gelatin composite nanofibers containing 30-40 wt.% of gelatin and electrospun in diluted acetic acid-ethyl acetate mixture produced nanofiber scaffolds with optimum hydrophilicity, degradability, and bio-functionality for stem cell-based bone tissue engineering.

  5. [Comparison of protective effects of eight ethyl acetate extracts from Eclipta prostrate on NHBE cells based on component structure theory].

    PubMed

    Ding, Shu-Min; Liu, Dan; Feng, Liang; Zhu, Fen-Xia; Tan, Xiao-Bin; Jia, Xiao-Bin

    2014-08-01

    To analyze and compare the protective effects of active components in different ethyl acetate extracts (EAEEPs) from Eclipta prostrate, in order to study the comparison of materials bases protecting normal human bronchial epithelial (NHBE) cells. The MTT assay was taken to compare the protective effect of different EAEEPs on cigarette smoke extracts (CSE) -induced NHBE cells. The ultra-performance liquid chromatography (UPLC) was applied to analyze the content of phenolic acid, coumaric grass ether and flavonoid in EAEEPs. According to the results, all of the eight EAEEPs (0-200 mg x L(-1)) showed certain protective effect on NHBE cells, with statistical difference. Specifically, the total mass of EAEEP VII (89.15 mg x L(-1)) and EAEEP VIII (57.44 mg x L(-1)), which showed the strongest activity, was not the highest, while EAEEP III (132.25 mg x L(-1)) displayed the highest total mass. In the combination with the "component structure" theory, the analysis showed a significant difference in the mass structure among phenolic acid, coumaric grass ether and flavonoid in EAEEP VIII and EAEEP VIII, which were 1.0: 1. 0: 0.5 and 1.0: 1.9: 0.8, respectively. The results suggested a specific optimal "component structure" relationship may exist in EAEEP, which could provide reference for the material base study and quality control.

  6. Inhibition of Hepatitis C Virus Replication and Viral Helicase by Ethyl Acetate Extract of the Marine Feather Star Alloeocomatella polycladia

    PubMed Central

    Yamashita, Atsuya; Salam, Kazi Abdus; Furuta, Atsushi; Matsuda, Yasuyoshi; Fujita, Osamu; Tani, Hidenori; Fujita, Yoshihisa; Fujimoto, Yuusuke; Ikeda, Masanori; Kato, Nobuyuki; Sakamoto, Naoya; Maekawa, Shinya; Enomoto, Nobuyuki; Nakakoshi, Masamichi; Tsubuki, Masayoshi; Sekiguchi, Yuji; Tsuneda, Satoshi; Akimitsu, Nobuyoshi; Noda, Naohiro; Tanaka, Junichi; Moriishi, Kohji

    2012-01-01

    Hepatitis C virus (HCV) is a causative agent of acute and chronic hepatitis, leading to the development of hepatic cirrhosis and hepatocellular carcinoma. We prepared extracts from 61 marine organisms and screened them by an in vitro fluorescence assay targeting the viral helicase (NS3), which plays an important role in HCV replication, to identify effective candidates for anti-HCV agents. An ethyl acetate-soluble fraction of the feather star Alloeocomatella polycladia exhibited the strongest inhibition of NS3 helicase activity, with an IC50 of 11.7 µg/mL. The extract of A. polycladia inhibited interaction between NS3 and RNA but not ATPase of NS3. Furthermore, the replication of the replicons derived from three HCV strains of genotype 1b in cultured cells was suppressed by the extract with an EC50 value of 23 to 44 µg/mL, which is similar to the IC50 value of the NS3 helicase assay. The extract did not induce interferon or inhibit cell growth. These results suggest that the unknown compound(s) included in A. polycladia can inhibit HCV replication by suppressing the helicase activity of HCV NS3. This study may present a new approach toward the development of a novel therapy for chronic hepatitis C. PMID:22690141

  7. Therapeutic effect of ethyl acetate extract from Asparagus cochinchinensis on phthalic anhydride-induced skin inflammation

    PubMed Central

    Sung, Ji-Eun; Lee, Hyun-Ah; Kim, Ji-Eun; Go, Jun; Seo, Eun-Ji; Yun, Woo-Bin; Kim, Dong-Seob; Son, Hong-Joo; Lee, Chung-Yeoul; Lee, Hee-Seob

    2016-01-01

    Asparagus cochinchinensis has been used to treat various diseases including fever, cough, kidney disease, breast cancer, inflammatory disease and brain disease, while IL-4 cytokine has been considered as key regulator on the skin homeostasis and the predisposition toward allergic skin inflammation. However, few studies have investigated its effects and IL-4 correlation on skin inflammation to date. To quantitatively evaluate the suppressive effects of ethyl acetate extracts of A. cochinchinensis (EaEAC) on phthalic anhydride (PA)-induced skin inflammation and investigate the role of IL-4 during their action mechanism, alterations in general phenotype biomarkers and luciferase-derived signals were measured in IL-4/Luc/CNS-1 transgenic (Tg) mice with PA-induced skin inflammation after treatment with EaEAC for 2 weeks. Key phenotype markers including lymph node weight, immunoglobulin E (IgE) concentration, epidermis thickness and number of infiltrated mast cells were significantly decreased in the PA+EaEAC treated group compared with the PA+Vehicle treated group. In addition, expression of IL-1β and TNF-α was also decreased in the PA+EaEAC cotreated group, compared to PA+Vehicle treated group. Furthermore, a significant decrease in the luciferase signal derived from IL-4 promoter was detected in the abdominal region, submandibular lymph node and mesenteric lymph node of the PA+EaEAC treated group, compared to PA+Vehicle treated group. Taken together, these results suggest that EaEAC treatment could successfully improve PA-induced skin inflammation of IL-4/Luc/CNS-1 Tg mice, and that IL-4 cytokine plays a key role in the therapeutic process of EaEAC. PMID:27051441

  8. Anticancer Effects of 1,3-Dihydroxy-2-Methylanthraquinone and the Ethyl Acetate Fraction of Hedyotis Diffusa Willd against HepG2 Carcinoma Cells Mediated via Apoptosis

    PubMed Central

    Li, Yun-lan; Zhang, Jiali; Min, Dong; Hongyan, Zhou; Lin, Niu; Li, Qing-shan

    2016-01-01

    Hedyotis Diffusa Willd, used in Traditional Chinese Medicine, is a treatment for various diseases including cancer, owing to its mild effectiveness and low toxicity. The aim of this study was to identify the main anticancer components in Hedyotis Diffusa Willd, and explore mechanisms underlying their activity. Hedyotis Diffusa Willd was extracted and fractionated using ethyl acetate to obtain the H-Ethyl acetate fraction, which showed higher anticancer activity than the other fractions obtained against HepG2 cells with sulforhodamine B assays. The active component of the H-Ethyl acetate fraction was identified to be 1,3-dihydroxy-2-methylanthraquinone (DMQ) with much high inhibitory rate up to 48.9 ± 3.3% and selectivity rate up to 9.4 ± 4.5 folds (p<0.01) at 125 μmol/L. HepG2 cells treated with the fraction and DMQ visualized morphologically using light and fluorescence microscopy. Annexin V—fluorescein isothiocyanate / propidium iodide staining flow cytometry, DNA ladder and cell cycle distribution assays. Mechanistic studies showed up-regulation of caspase-3, -8, and -9 proteases activities (p<0.001), indicating involvement of mitochondrial apoptotic and death receptor pathways. Further studies revealed that reactive oxygen species in DMQ and the fraction treated HepG2 cells increased (p<0.01) while mitochondrial membrane potential reduced significantly (p<0.001) compared to the control by flow cytometry assays. Western blot analysis showed that Bax, p53, Fas, FasL, p21 and cytoplasmic cytochrome C were up-regulated (p<0.01), while Bcl-2, mitochondrial cytochrome C, cyclin E and CDK 2 were down-regulated dose-dependently (p<0.01). The reverse transcriptase-polymerase chain reaction showed that mRNA expressions of p53 and Bax increased (p<0.001) while that of Bcl-2 decreased (p<0.001). Pre-treatment with caspase-8 inhibitor Z-IETD-FMK, or caspase-9 inhibitor Z-LEHD-FMK, attenuated the growth-inhibitory and apoptosis-inducing effects of DMQ and the fraction

  9. Cellular Anti-Melanogenic Effects of a Euryale ferox Seed Extract Ethyl Acetate Fraction via the Lysosomal Degradation Machinery

    PubMed Central

    Baek, Seung-Hwa; Nam, In-Jeong; Kwak, Hyeong Seob; Kim, Ki-Chan; Lee, Sang-Han

    2015-01-01

    The aim of this study was to investigate the effect of ethyl acetate fraction of Euryale ferox seed extracts (Efse-EA) on melanogenesis in immortalized mouse melanocyte cell line, melan-a. Efse-EA showed strong dose-dependent mushroom tyrosinase inhibitory activity. Treatment of melan-a cells with 30 μg/mL Efse-EA produced strong inhibition of cellular tyrosinase and melanin synthesis. Efse-EA significantly reduced the levels of melanogenesis-related proteins, such as tyrosinase, tyrosinase-related proteins 1 and 2, and microphthalmia-associated transcription factor. Because Efse-EA treatment reduced tyrosinase protein levels without changing its mRNA expression, we investigated whether this decrease was related to proteasomal or lysosomal degradation of tyrosinase. We found that chloroquine, a lysosomal proteolysis inhibitor, almost completely abolished both the down-regulation of tyrosinase and the inhibition of melanin synthesis induced by Efse-EA. These results suggested that Efse-EA may contribute to the inhibition of melanogenesis by altering lysosomal degradation of tyrosinase, and that this extract may provide a new cosmetic skin-whitening agent. PMID:25915032

  10. Cellular Anti-Melanogenic Effects of a Euryale ferox Seed Extract Ethyl Acetate Fraction via the Lysosomal Degradation Machinery.

    PubMed

    Baek, Seung-Hwa; Nam, In-Jeong; Kwak, Hyeong Seob; Kim, Ki-Chan; Lee, Sang-Han

    2015-04-23

    The aim of this study was to investigate the effect of ethyl acetate fraction of Euryale ferox seed extracts (Efse-EA) on melanogenesis in immortalized mouse melanocyte cell line, melan-a. Efse-EA showed strong dose-dependent mushroom tyrosinase inhibitory activity. Treatment of melan-a cells with 30 μg/mL Efse-EA produced strong inhibition of cellular tyrosinase and melanin synthesis. Efse-EA significantly reduced the levels of melanogenesis-related proteins, such as tyrosinase, tyrosinase-related proteins 1 and 2, and microphthalmia-associated transcription factor. Because Efse-EA treatment reduced tyrosinase protein levels without changing its mRNA expression, we investigated whether this decrease was related to proteasomal or lysosomal degradation of tyrosinase. We found that chloroquine, a lysosomal proteolysis inhibitor, almost completely abolished both the down-regulation of tyrosinase and the inhibition of melanin synthesis induced by Efse-EA. These results suggested that Efse-EA may contribute to the inhibition of melanogenesis by altering lysosomal degradation of tyrosinase, and that this extract may provide a new cosmetic skin-whitening agent.

  11. Ethyl acetate extract of Hypericum japonicum induces apoptosis via the mitochondria-dependent pathway in vivo and in vitro.

    PubMed

    Zhuang, Qunchuan; Li, Jing; Chen, Youqin; Lin, Jiumao; Lai, Faze; Chen, Xuzheng; Lin, Xindeng; Peng, Jun

    2015-10-01

    The widely-used Chinese medicinal herb Hypericum japonicum, also known as Hypericum japonicum Thunb or Tianjihuang, displays potent anti‑carcinogenic effects against liver cancer. However, the molecular mechanism underlying the therapeutic effects of Hypericum japonicum remains to be elucidated. The present study investigated the in vivo efficacy of ethyl acetate extract of Hypericum japonicum (EAEHJ) against tumor growth in an H22 cell‑bearing liver cancer mouse model. Treatment with EAEHJ significantly reduced tumor weight, but had no effect on murine body weight. The results of the present study also showed that EAEHJ induced H22 cell apoptosis in vivo. In addition, the anti‑carcinogenic effects of EAEHJ were investigated in vitro. The results of the present study demonstrate that both phospholipid asymmetry in the plasma membrane and mitochondrial membrane potential were deregulated in HepG2 human hepatoma cells, following treatment with EAEHJ. Treatment with EAEHJ also increased the ratio of pro‑apoptotic B‑cell lymphoma 2 (Bcl‑2)‑associated X protein (Bax) to anti‑apoptotic Bcl‑2, and activated the caspase‑9 signaling pathway. These results suggest that EAEHJ is able to trigger the apoptosis of liver cancer cells via the mitochondria-dependent pathway.

  12. Ethyl acetate extract of Peperomia tetraphylla induces cytotoxicity, cell cycle arrest, and apoptosis in lymphoma U937 cells.

    PubMed

    Yu, Dayong; Yang, Xiuxiu; Lu, Xuan; Shi, Liying; Feng, Baomin

    2016-12-01

    The current study evaluated the cytotoxicity and the mechanism of apoptotic induction by Peperomia tetraphylla in U937 lymphoma cells. The results showed that P. tetraphylla ethyl acetate extract (EAEPT) inhibited the cell growth in U937 cells by MTT assay. After the U937 cells were treated with EAEPT, the cells exhibited marked morphological features of apoptosis (Hoechst 33342 staining) and the number of apoptotic cell (Annexin V-FITC/PI staining) increased. The treatment of EAEPT could induce loss of mitochondrial membrane potential (MMP) and increase the ROS level. Moreover, EAEPT treatment resulted in the accumulation of cells at S phase. We found that EAEPT could induce the cleavage of the caspase 3, caspase 8, caspase 9 and Bid. And the treatment of EAEPT could increase expression of Bax and down-regulate the expression of CCNB1, CCND1 and CDK1. The sub-fraction of EAEPT, namely EASub1 demonstrated the highest cytotoxicity activity on U937 cells. It was confirmed that EAEPT could inhibit the growth of U937 cells by blocking the cell cycle and prompted apoptosis via the ROS-medicated mitochondria pathway in vitro.

  13. Diabetic therapeutic effects of ethyl acetate fraction from the roots of Musa paradisiaca and seeds of Eugenia jambolana in streptozotocin-induced male diabetic rats.

    PubMed

    Panda, D K; Ghosh, Debidas; Bhat, B; Talwar, S K; Jaggi, M; Mukherjee, R

    2009-11-01

    The folklore medicine of primitive people has been greatly appreciated for centuries. Many researchers study the curative efficiency and mode of action of various medicinal plants. Serum glucose level, lipid profile, glucose tolerance, hepatic and muscle glycogen contents as well as the activities of hepatic hexokinase and glucose-6-phosphatase recovered significantly after oral administration of ethyl acetate fractions of Eugenia jambolana (E. jambolana) or Musa paradisiaca (M. paradisiaca) in separate (E. jambolana L.: 200 mg/kg of body weight and M. paradisiaca: 100 mg/kg of body weight) or combined form for 90 days (twice a day through gavage) to streptozotocin-induced diabetic rats. The loss in body weight of diabetic animals was reversed and serum levels of insulin as well as C-peptide, which were found to be reduced in diabetic rats, increased significantly after oral administration of the fractions. A histological study of the rats' pancreas revealed that after 90 days of oral treatment with the plant fractions in separate or combined form, the size and volume of pancreatic islets in diabetic treated rats increased significantly compared with the diabetic control group. Treatment of diabetic rats with the combined dose (300 mg/kg of body weight) of plant fractions (200 mg E. jambolana and 100 mg M. paradisiaca) was found to be more effective than treatment with the individual fraction. The doses of E. jambolana and M. paradisiaca selected for this study are the optimum antihyperglycemic doses of the plant fractions, which were determined after conducting a dose-dependent study at various dose levels (50-500 mg/kg) in our pilot experiments. The plant fractions were found to be free from metabolic toxicity. Through HPTLC finger printing, three different compounds were noted in the ethyl acetate fraction of E. jambolana L. and eight different compounds in the ethyl acetate fraction of M. paradisiaca L.

  14. Harpagophytum Procumbens Ethyl Acetate Fraction Reduces Fluphenazine-Induced Vacuous Chewing Movements and Oxidative Stress in Rat Brain.

    PubMed

    Schaffer, Larissa Finger; de Freitas, Catiuscia Molz; Chiapinotto Ceretta, Ana Paula; Peroza, Luis Ricardo; de Moraes Reis, Elizete; Krum, Bárbara Nunes; Busanello, Alcindo; Boligon, Aline Augusti; Sudati, Jéssie Haigert; Fachinetto, Roselei; Wagner, Caroline

    2016-05-01

    Long-term treatment with fluphenazine is associated with manifestation of extrapyramidal side effects, such as tardive dyskinesia. The molecular mechanisms related to the pathophysiology of TD remain unclear, and several hypotheses, including a role for oxidative stress, have been proposed. Harpagophytum procumbens is an herbal medicine used mainly due to anti-inflammatory effects, but it also exhibits antioxidant effects. We investigated the effect of ethyl acetate fraction of H. procumbens (EAF HP) in fluphenazine-induced orofacial dyskinesia by evaluating behavioral parameters at different times (vacuous chewing movements (VCM's) and locomotor and exploratory activity), biochemical serological analyses, and biochemical markers of oxidative stress of the liver, kidney, cortex, and striatum. Chronic administration of fluphenazine (25 mg/kg, intramuscular (i.m) significantly increased the VCMs at all analyzed times (2, 7, 14, and 21 days), and this was inhibited by EAF HP (especially at a dose of 30 mg/kg). Fluphenazine decreased locomotion and exploratory activity, and EAF HP did not improve this decrease. Fluphenazine induced oxidative damage, as identified by changes in catalase activity and ROS levels in the cortex and striatum, which was reduced by EAF HP, especially in the striatum. In the cortex, EAF HP was protective against fluphenazine-induced changes in catalase activity but not against the increase in ROS level. Furthermore, EAF HP was shown to be safe, since affected serum biochemical parameters or parameters of oxidative stress in the liver and kidney. These findings suggest that the H. procumbens is a promising therapeutic agent for the treatment of involuntary oral movements.

  15. Field study of the urinary excretion of ethoxyacetic acid during repeated daily exposure to the ethyl ether of ethylene glycol and the ethyl ether of ethylene glycol acetate.

    PubMed

    Veulemans, H; Groeseneken, D; Masschelein, R; Van Vlem, E

    1987-06-01

    The urinary excretion of ethoxyacetic acid (EAA) was studied in a group of five women daily exposed to the ethyl ether of ethylene glycol (EGEE) and the ethyl ether of ethylene glycol acetate (EGEE-Ac) during 5 d of normal production and 7 d after a 12-d production stop. The mean combined exposure concentration of EGEE and EGEE-Ac (expressed in equivalent weight of EGEE) was 14.0 mg/m3 with occasional slight excursions above the current Belgian occupational exposure limit. The daily combined exposure profiles for EGEE and EGEE-Ac were rather constant during the first observation period, but they tended to decrease during the last week. The urinary EAA excretion clearly increased during the work week. Over the weekends the elimination was far from complete, and even after a prolonged nonexposure period of 12 d traces of the metabolite were still detectable. Based on the observations from the first period, a good linear correlation (r = 0.92) was found between the average exposure over 5 d (14.4 mg/m3) and the EAA excretion at the end of the week (105.7 mg/g creatinine). An EAA estimate of 150 +/- 35 mg/g was found to correspond with repeated 5-d full-shift exposures to the respective occupational exposure limit of EGEE (19 mg/m3) or EGEE-Ac (27 mg/m3).

  16. 1-Ethyl-3-methylimidazolium acetate as a highly efficient organocatalyst for cyanosilylation of carbonyl compounds with trimethylsilyl cyanide

    PubMed Central

    Ullah, Bakhtar; Chen, Jingwen; Zhang, Zhiguo; Xing, Huabin; Yang, Qiwei; Bao, Zongbi; Ren, Qilong

    2017-01-01

    1-Ethyl-3-methylimidazolium acetate is introduced as a robust organocatalyst for solvent-free cyanosilylation of carbonyl compounds with trimethylsilyl cyanide (TMSCN). The catalyst loading can be reduced to as low as 0.1–0.0001 mol % under mild reaction conditions, giving considerably high TOF values from 10,843 h−1 to 10,602,410 h−1 in the field of organocatalyzed transformations. The present protocol not only tolerates with extensive carbonyl compounds but also provides somewhat insight into the mechanism of ionic liquids (ILs)-catalyzed reactions. PMID:28198462

  17. 1-Ethyl-3-methylimidazolium acetate as a highly efficient organocatalyst for cyanosilylation of carbonyl compounds with trimethylsilyl cyanide

    NASA Astrophysics Data System (ADS)

    Ullah, Bakhtar; Chen, Jingwen; Zhang, Zhiguo; Xing, Huabin; Yang, Qiwei; Bao, Zongbi; Ren, Qilong

    2017-02-01

    1-Ethyl-3-methylimidazolium acetate is introduced as a robust organocatalyst for solvent-free cyanosilylation of carbonyl compounds with trimethylsilyl cyanide (TMSCN). The catalyst loading can be reduced to as low as 0.1–0.0001 mol % under mild reaction conditions, giving considerably high TOF values from 10,843 h‑1 to 10,602,410 h‑1 in the field of organocatalyzed transformations. The present protocol not only tolerates with extensive carbonyl compounds but also provides somewhat insight into the mechanism of ionic liquids (ILs)-catalyzed reactions.

  18. Ethyl Acetate Extract of Origanum vulgare L. ssp. hirtum Prevents Streptozotocin-Induced Diabetes in C57BL/6 Mice.

    PubMed

    Vujicic, Milica; Nikolic, Ivana; Kontogianni, Vassiliki G; Saksida, Tamara; Charisiadis, Pantelis; Vasic, Bobana; Stosic-Grujicic, Stanislava; Gerothanassis, Ioannis P; Tzakos, Andreas G; Stojanovic, Ivana

    2016-07-01

    Type 1 diabetes (T1D) is an autoimmune disease that develops as a consequence of pancreatic β-cell death induced by proinflammatory mediators. Because Origanum vulgare L. ssp. hirtum (Greek oregano) contains antiinflammatory molecules, we hypothesized that it might be beneficial for the treatment of T1D. An ethyl acetate extract of oregano (EAO) was prepared from the leaves by a polar extraction method. Phytochemical composition was determined by liquid chromatography-UV diode array coupled to ion-trap mass spectrometry with electrospray ionization interface (LC/DAD/ESI-MS(n) ). In vitro immunomodulatory effect of EAO was estimated by measuring proliferation (MTT) or cytokine secretion (ELISA) from immune cells. Diabetes was induced by multiple low doses of streptozotocin (MLDS) in male C57BL/6 mice and EAO was administered intraperitoneally for 10 d. Determination of cellular composition (flow cytometry) and cytokine production (ELISA) was performed on 12th d after diabetes induction. EAO suppressed the function of both macrophages and lymphocytes in vitro. In vivo, EAO treatment significantly preserved pancreatic islets and reduced diabetes incidence in MLDS-challenged mice. Besides down-modulatory effect on macrophages, EAO reduced the number of total CD4(+) and activated CD4(+) CD25(+) T cells. Furthermore, EAO affected the number of T helper 1 (Th1) and T helper 17 (Th17) cells through downregulation of their key transcription factors T-bet and RORγT. Because EAO treatment protects mice from development of hyperglycemia by reducing proinflammatory macrophage/Th1/Th17 response, this plant extract could represent a basis for future diabetes therapy.

  19. High throughput, colorimetric screening of microbial ester biosynthesis reveals high ethyl acetate production from Kluyveromyces marxianus on C5, C6, and C12 carbon sources.

    PubMed

    Löbs, Ann-Kathrin; Lin, Jyun-Liang; Cook, Megan; Wheeldon, Ian

    2016-10-01

    Advances in genome and metabolic pathway engineering have enabled large combinatorial libraries of mutant microbial hosts for chemical biosynthesis. Despite these advances, strain development is often limited by the lack of high throughput functional assays for effective library screening. Recent synthetic biology efforts have engineered microbes that synthesize acetyl and acyl esters and many yeasts naturally produce esters to significant titers. Short and medium chain volatile esters have value as fragrance and flavor compounds, while long chain acyl esters are potential replacements for diesel fuel. Here, we developed a biotechnology method for the rapid screening of microbial ester biosynthesis. Using a colorimetric reaction scheme, esters extracted from fermentation broth were quantitatively converted to a ferric hydroxamate complex with strong absorbance at 520 nm. The assay was validated for ethyl acetate, ethyl butyrate, isoamyl acetate, ethyl hexanoate, and ethyl octanoate, and achieved a z-factor of 0.77. Screening of ethyl acetate production from a combinatorial library of four Kluyveromyces marxianus strains on seven carbon sources revealed ethyl acetate biosynthesis from C5, C6, and C12 sugars. This newly adapted method rapidly identified novel properties of K. marxianus metabolism and promises to advance high throughput microbial strain engineering for ester biosynthesis.

  20. Antiamnesic effects of ethyl acetate fraction from chestnut (Castanea crenata var. dulcis) inner skin on Aβ(25-35)-induced cognitive deficits in mice.

    PubMed

    Jeong, Hee-Rok; Jo, Yu Na; Jeong, Ji Hee; Jin, Dong Eun; Song, Byung Gi; Choi, Soo Jung; Shin, Dong-Hoon; Heo, Ho Jin

    2012-12-01

    To investigate neuronal cell protective effects of an ethyl acetate fraction from chestnut inner skin, in vitro assays, including 2',7'-dichlorofluorescein diacetate, 3-[4,5-dimethythiazol-2-yl]-2,5-diphenyl tetrazolium bromide (MTT), and lactate dehydrogenase (LDH), were performed. Intracellular accumulation of reactive oxygen species resulting from hydrogen peroxide (H(2)O(2)) treatment of PC12 cells was significantly reduced when ethyl acetate fractions were present in the medium compared to PC12 cells treated with H(2)O(2) only. In a cell viability assay using MTT, the ethyl acetate fraction protected against H(2)O(2)-induced neurotoxicity, and inhibited LDH release into the medium. In addition, the ethyl acetate fraction improved in vivo cognitive ability against amyloid β-peptide (Aβ)-induced neuronal deficit. High-performance liquid chromatography analyses showed that gallic acid, catechin, and epicatechin were predominant phenolics in the ethyl acetate fraction. Consequently, the results suggest that chestnut inner skin, including above phenolics, could ameliorate Aβ-induced learning and memory deficiency, and be utilized as effective substances for neurodegenerative disorders, notably Alzheimer's disease.

  1. Ethyl Acetate Extracts of Semen Impatientis Inhibit Proliferation and Induce Apoptosis of Human Prostate Cancer Cell Lines through AKT/ERK Pathways.

    PubMed

    Wang, Tao; Cai, Yang; Song, Wen; Chen, Ruibao; Hu, Dunmei; Ye, Jianhan; Liu, Lu; Peng, Wei; Zhang, Junfeng; Wang, Shaogang; Yang, Weiming; Liu, Jihong; Ding, Yufeng

    2017-01-01

    Objective. To investigate the inhibitory effect of ethyl acetate extracts of Impatiens balsamina L. on prostate cancer cells. Methods. Impatiens balsamina L. was extracted to get water, ethanol, oil ether, ethyl acetate, and butanol extracts. CCK-8 assay was used to detect the inhibitory effect. Apoptosis rates and cell cycle distribution were detected by flow cytometry. Transwell assay was performed to test the ability of migration. The expressions of Bcl-2, Bax, cleaved-caspase-3, p-ERK, ERK, p-AKT, AKT, cyclin D1, cyclin E, and MMP2 were detected by Western blot. Results. Ethyl acetate extracts had the strongest inhibitory effect. After being treated with different concentrations of ethyl acetate extracts, the percentage of G0/G1 phase increased significantly, cyclin D1 and cyclin E expression decreased, apoptosis rate was significantly higher, and the ability of migration of PC-3 and RV1 was inhibited significantly. Western blot showed that the expressions of Bcl-2, p-ERK, and p-AKT were significantly decreased, but the expressions of Bax and caspase-3 cleavage were increased. Conclusions. Impatiens balsamina L. inhibited the proliferation of human prostate cancer cells; ethyl acetate extracts have the strongest effect. It could inhibit cell proliferation and migration, cause G1 phase arrest, and induce apoptosis probably through inhibition of the AKT and ERK pathways.

  2. Ethyl Acetate Extracts of Semen Impatientis Inhibit Proliferation and Induce Apoptosis of Human Prostate Cancer Cell Lines through AKT/ERK Pathways

    PubMed Central

    Wang, Tao; Cai, Yang; Song, Wen; Chen, Ruibao; Hu, Dunmei; Ye, Jianhan; Liu, Lu; Peng, Wei; Zhang, Junfeng; Yang, Weiming; Liu, Jihong

    2017-01-01

    Objective. To investigate the inhibitory effect of ethyl acetate extracts of Impatiens balsamina L. on prostate cancer cells. Methods. Impatiens balsamina L. was extracted to get water, ethanol, oil ether, ethyl acetate, and butanol extracts. CCK-8 assay was used to detect the inhibitory effect. Apoptosis rates and cell cycle distribution were detected by flow cytometry. Transwell assay was performed to test the ability of migration. The expressions of Bcl-2, Bax, cleaved-caspase-3, p-ERK, ERK, p-AKT, AKT, cyclin D1, cyclin E, and MMP2 were detected by Western blot. Results. Ethyl acetate extracts had the strongest inhibitory effect. After being treated with different concentrations of ethyl acetate extracts, the percentage of G0/G1 phase increased significantly, cyclin D1 and cyclin E expression decreased, apoptosis rate was significantly higher, and the ability of migration of PC-3 and RV1 was inhibited significantly. Western blot showed that the expressions of Bcl-2, p-ERK, and p-AKT were significantly decreased, but the expressions of Bax and caspase-3 cleavage were increased. Conclusions. Impatiens balsamina L. inhibited the proliferation of human prostate cancer cells; ethyl acetate extracts have the strongest effect. It could inhibit cell proliferation and migration, cause G1 phase arrest, and induce apoptosis probably through inhibition of the AKT and ERK pathways. PMID:28386546

  3. Determination of permeation parameters of experimental PET films coated with SiOx to ethyl acetate, oxygen and water vapour.

    PubMed

    Adamantiadi, A; Badeka, A; Kontominas, M G

    2001-11-01

    The permeation parameters of conventional PET films, films coated with SiOx and SiOx-coated films laminated to LDPE were determined for ethyl acetate using the permeation cell/gas chromatography method. Permeation to O2 and water vapour was also determined to monitor overall changes in the barrier properties of the experimental films. Coating of the PET film was achieved by a 'directed evaporation' method that increased the yield of the coating process from 30-35 to > 70%. It was shown that the SiOx coating increased the film barrier to ethyl acetate by approximately 20-30 times. Permeation values showed low reproducibility, indicating the need for further development and standardization of the 'directed evaporation' web-coating process. The barrier to oxygen and water vapour increased by 20-25 and 12-14 times respectively after coating. The web-coating speed did not seem to influence the barrier properties of the films. Permeation coefficients, diffusion coefficients and solubility coefficients were calculated for all samples.

  4. Template-assisted hydrothermally obtained titania-ceria composites and their application as catalysts in ethyl acetate oxidation and methanol decomposition with a potential for sustainable environment protection

    NASA Astrophysics Data System (ADS)

    Tsoncheva, Tanya; Mileva, Alexandra; Issa, Gloria; Dimitrov, Momtchil; Kovacheva, Daniela; Henych, Jiří; Scotti, Nicola; Kormunda, Martin; Atanasova, Genoveva; Štengl, Vaclav

    2017-02-01

    High surface area mesoporous ceria-titania binary materials with high Lewis acidity and improved reduction properties were synthesized using template assisted hydrothermal technique. The obtained materials were characterized by low temperature nitrogen physisorption, XRD, SEM, TEM, Raman, UV-vis, XPS, FTIR, FTIR of adsorbed pyridine and thermo-programmed reduction with hydrogen. Their catalytic activity was tested in total oxidation of ethyl acetate and methanol decomposition to CO and hydrogen with a potential application in VOCs elimination and alternative fuels, respectively. The structural changes in the binary materials, which could be tuned by the variation in the Ce/Ti ratio and the temperature of hydrothermal treatment, provoked significant changes in their textural, surface and redox properties, which is in close relation to the catalytic activity and selectivity in various catalytic processes. The intimate contact between the individual oxides results in the formation of different catalytic active sites and their role in the studied catalytic reactions was discussed in details.

  5. Ethyl 2-acetyl­hydrazono-2-phenyl­acetate

    PubMed Central

    Xu, Liang-Zhong; Yi, Xu; An, Guang-Wei; Zhang, Gong-Sheng; Li, Chun-Fang

    2008-01-01

    The title compound, C12H14N2O3, was synthesized as an inter­mediate for the synthesis of metamitron. The benzene ring forms dihedral angles of 86.3 (2) and 10.0 (3)° with the ethyl group and the acetyl­imino plane, respectively. The crystal structure involves inter­molecular C—H⋯O and N—H⋯O hydrogen bonds. PMID:21200890

  6. Effect of the ionic liquid 1-ethyl-3-methylimidazolium acetate on the phase transition of starch: dissolution or gelatinization?

    PubMed

    Mateyawa, Sainimili; Xie, David Fengwei; Truss, Rowan W; Halley, Peter J; Nicholson, Timothy M; Shamshina, Julia L; Rogers, Robin D; Boehm, Michael W; McNally, Tony

    2013-04-15

    This work revealed that the interactions between starch, the ionic liquid 1-ethyl-3-methylimidazolium acetate ([Emim][OAc]), and water might contribute to the phase transition (gelatinization, dissolution, or both) of native starch at reduced temperature. Using mixtures of water and [Emim][OAc] at certain ratios (7.2/1 and 10.8/1 mol/mol), both the gelatinization and dissolution of the starch occur competitively, but also in a synergistic manner. At lower [Emim][OAc] concentration (water/[Emim][OAc] molar ratio≥25.0/1), mainly gelatinization occurs which is slightly impeded by the strong interaction between water and [Emim][OAc]; while at higher [Emim][OAc] concentration (water/[Emim][OAc] molar ratio≤2.8/1), the dissolution of starch is the major form of phase transition, possibly restricted by the difficulty of [Emim][OAc] to interact with starch.

  7. Development of cellulose acetate propionate membrane for separation of ethanol and ethyl tert-butyl ether mixtures

    SciTech Connect

    Luo, G.S.; Niang, M.; Schaetzel, P.

    1997-04-01

    For pervaporation separation of ethanol and ethyl tert-butyl ether mixtures, a cellulose acetate propionate membrane was chosen as the experimental membrane because of its high selectivity and good mass fluxes. The properties of the membranes were evaluated by the pervaporation separation of mixtures of ethyl tert-butyl ether/ethanol and the sorption experiments. The experimental results showed that the selectivity and the permeates depend on the ethanol concentration in the feed and the experimental temperature. With increases of the ethanol weight fraction in the feed and the temperature, the total and partial mass fluxes increased. With respect to the temperature, ethanol mass flux obeys the Arrhenius equation. The selectivity of this membrane decreases as the temperature and the ethanol concentration in the feed increase. This membrane shows special characteristics at the azeotropic composition. In the vicinity of the azeotropic point, minimum values of ethanol concentration in the permeate and in sorption solution are obtained. The swelling ratios increase when temperature and the ethanol concentration in the feed are increasing. The ethanol concentration in the sorption solution is also influenced by the temperature and the mixture`s composition. When the temperature increases, the sorption selectivity of the membrane decreases.

  8. Ethyl acetate extract from Asparagus cochinchinensis exerts anti‑inflammatory effects in LPS‑stimulated RAW264.7 macrophage cells by regulating COX‑2/iNOS, inflammatory cytokine expression, MAP kinase pathways, the cell cycle and anti-oxidant activity.

    PubMed

    Lee, Hyun Ah; Koh, Eun Kyoung; Sung, Ji Eun; Kim, Ji Eun; Song, Sung Hwa; Kim, Dong Seob; Son, Hong Joo; Lee, Chung Yeoul; Lee, Hee Seob; Bae, Chang Joon; Hwang, Dae Youn

    2017-04-01

    Asparagus cochinchinesis (A. cochinchinesis) is a medicine traditionally used to treat fever, cough, kidney disease, breast cancer, inflammatory disease and brain disease in northeast Asian countries. Although numerous studies of the anti‑inflammatory effects of A. cochinchinesis have been conducted, the underlying mechanisms of such effects in macrophages remain to be demonstrated. To investigate the mechanism of suppressive effects on the inflammatory response in macrophages, alterations of the nitric oxide (NO) level, the cell viability, inducible nitric oxide synthase (iNOS) and cyclooxygenase‑2 (COX‑2) expression levels, inflammatory cytokine expression, the mitogen-activated protein kinase (MAPK) signaling pathway, cell cycle arrest and reactive oxygen species (ROS) levels were measured in lipopolysaccharide (LPS)-activated RAW264.7 cells following treatment with ethyl acetate extract from A. cochinchinesis root (EaEAC). RAW264.7 cells pretreated two different concentrations of EaEAC prior to LPS treatment exhibited no significant toxicity. The concentration of NO was significantly decreased in the EaEAC + LPS treated group compared with the vehicle + LPS treated group. A similar decrease in mRNA transcript level of COX‑2, iNOS, pro-inflammatory cytokines [tumor necrosis factor‑α and interleukin (IL)‑1β] and anti‑inflammatory cytokines (IL‑6 and IL‑10) was detected in the EaEAC + LPS treated group compared with the vehicle + LPS treated group, although the decrease rate varied. Enhancement of the phosphorylation of MAPK family members following LPS treatment was partially rescued in the EaEAC pretreated group, and the cell cycle was arrested at the G2/M phase. Furthermore, the EaEAC pretreated group exhibited a reduced level of ROS generation compared with the vehicle + LPS treated group. Taken together, these results suggest that EaEAC suppresses inflammatory responses through inhibition of NO production, COX‑2 expression

  9. Hypoglycemic Effect of Ethanol and Ethyl Acetate Extract of Phellinus baumii Fruiting Body in Streptozotocin-Induced Diabetic Mice

    PubMed Central

    Wang, Wen-Han; Wu, Fei-Hua; Yang, Yan; Wu, Na; Zhang, Jing-Song; Feng, Na; Tang, Chuan-Hong

    2015-01-01

    We investigated hypoglycemic effect of ethanol (EtOH) and ethyl acetate extract acetate (AcOEt) extracts in streptozotocin- (STZ-) induced diabetic mice. Our data showed the maximum inhibitory effect on the fasting plasma glucose (FPG) level was detected in STZ-induced diabetic mice administered with 400 mg/kg AcOEt extract of P. baumii. A lower glycated albumin (GA) level and a higher insulin level were observed in 400 mg/kg AcOEt and EtOH extract groups. Moreover, 400 mg/kg AcOEt and EtOH extract exhibited a stronger effect on increasing size and cell number of islets. The insulin expression level of β-cells and integrated optical density (IOD) value were significantly increased by the administration of 400 mg/kg AcOEt and EtOH extracts. Taken together, AcOEt and EtOH extracts of P. baumii fruiting body exhibited considerable hypoglycemic effect on STZ-induced diabetic mice. PMID:26221177

  10. Mixtures of the 1-ethyl-3-methylimidazolium acetate ionic liquid with different inorganic salts: insights into their interactions.

    PubMed

    Oliveira, Filipe S; Cabrita, Eurico J; Todorovic, Smilja; Bernardes, Carlos E S; Lopes, José N Canongia; Hodgson, Jennifer L; MacFarlane, Douglas R; Rebelo, Luís P N; Marrucho, Isabel M

    2016-01-28

    In this work, we explore the interactions between the ionic liquid 1-ethyl-3-methylimidazolim acetate and different inorganic salts belonging to two different cation families, those based on ammonium and others based on sodium. NMR and Raman spectroscopy are used to screen for changes in the molecular environment of the ions in the ionic liquid + inorganic salt mixtures as compared to pure ionic liquid. The ion self-diffusion coefficients are determined from NMR data, allowing the discussion of the ionicity values of the ionic liquid + inorganic salt mixtures calculated using different methods. Our data reveal that preferential interactions are established between the ionic liquid and ammonium-based salts, as opposed to sodium-based salts. Computational calculations show the formation of aggregates between the ionic liquid and the inorganic salt, which is consistent with the spectroscopic data, and indicate that the acetate anion of the ionic liquid establishes preferential interactions with the ammonium cation of the inorganic salts, leaving the imidazolium cation less engaged in the media.

  11. Relative Study of Luminescent Properties with Judd-Ofelt Characterization in Trivalent Europium Complexes Comprising ethyl-(4-fluorobenzoyl) Acetate.

    PubMed

    Devi, Rekha; Chahar, Sangeeta; Khatkar, S P; Taxak, V B; Boora, Priti

    2017-03-13

    Five new europium(III) complexes Eu(p-EFBA)3.(H2O)2 (C1), Eu(p-EFBA)3.neo (C2), Eu(p-EFBA)3.batho (C3), Eu(p-EFBA)3.phen (C4), Eu(p-EFBA)3.bipy (C5) have been synthesized by using ethyl-(4-fluorobenzoyl) acetate (p-EFBA) as β-ketoester ligand and neocuproine (neo), bathophenanthroline (batho), 1,10-phenanthroline (phen) and 2,2-bipyridyl (bipy) as ancillary ligands. The synthesized complexes C1-C5 were characterized by elemental analysis, nuclear magnetic resonance spectroscopy ((1)H-NMR), infrared (IR) spectroscopy, thermogravimetric analysis (TG/DTG), UV-visible and photoluminescence (PL) spectroscopy. The relative study of luminescence spectra of complexes with the previously reported complexes of isomeric ligand (ortho and meta substituted ligand) indicate the higher luminescence properties of complexes as an effect of fluorine position on β-ketoester ligand. The para substituted ligand shows a remarkable effect on quantum efficiencies and Judd-Ofelt intensity parameters (Ω2, Ω4) of the complexes. The higher value of intensity parameter Ω2 associated with hypersensitive (5)D0 → (7)F2 transition of europium(III) ion revealing highly polarizable ligand field. The purposed energy transfer mechanism of complexes indicates the efficient energy transfer in complexes.

  12. Characteristics of starch-based films with different amylose contents plasticised by 1-ethyl-3-methylimidazolium acetate.

    PubMed

    Xie, Fengwei; Flanagan, Bernadine M; Li, Ming; Truss, Rowan W; Halley, Peter J; Gidley, Michael J; McNally, Tony; Shamshina, Julia L; Rogers, Robin D

    2015-05-20

    Starch-based films plasticised by an ionic liquid, 1-ethyl-3-methylimidazolium acetate ([Emim][OAc]), were prepared by a simple compression moulding process, facilitated by the strong plasticisation effect of [Emim][OAc]. The effects of amylose content of starch (regular vs. high-amylose maize) and relative humidity (RH) during ageing of the samples on a range of structural and material characteristics were investigated. Surprisingly, plasticisation by [Emim][OAc] made the effect of amylose content insignificant, contrary to most previous studies when other plasticisers were used. In other words, [Emim][OAc] changed the underlying mechanism responsible for mechanical properties from the entanglement of starch macromolecules (mainly amylose), which has been reported as a main responsible factor previously. The crystallinity of the plasticised starch samples was low and thus was unlikely to have a major contribution to the material characteristics, although the amylose content impacted on the crystalline structure and the mobility of amorphous parts in the samples to some extent. Therefore, RH conditioning and thus the sample water content was the major factor influencing the mechanical properties, glass transition temperature, and electrical conductivity of the starch films. This suggests the potential application of ionic liquid-plasticised starch materials in areas where the control of properties by environmental RH is desired.

  13. Michrochip chromatography using an open-tubular microchannel and a ternary water-ACN-ethyl acetate mixture carrier solution.

    PubMed

    Matsuda, Takafumi; Yamashita, Kenichi; Maeda, Hideaki; Hashimoto, Masahiko; Tsukagoshi, Kazuhiko

    2013-03-01

    A capillary chromatography system has been developed using a ternary mixed-solvents solution, i.e. water-hydrophilic/hydrophobic organic solvent mixture as a carrier solution. Here, we tried to carry out the chromatographic system on a microchip incorporating the open-tubular microchannels. A model analyte solution of isoluminol isothiocyanate (ILITC) and ILITC-labeled biomolecule was injected to the double T-junction part on the microchip. The analyte solution was delivered in the separation microchannel (40 μm deep, 100 μm wide, and 22 cm long) with the ternary water-ACN-ethyl acetate mixture carrier solution (3:8:4 volume ratio, the organic solvent rich or 15:3:2 volume ratio, the water-rich). The analyte, free-ILITC and labeled BSA mixture, was separated through the microchannel, where the carrier solvents were radially distributed in the separation channel generating inner and outer phases. The outer phase acts as a pseudo-stationary phase under laminar flow conditions in the system. The ILITC and the labeled BSA were eluted and detected with chemiluminescence reaction.

  14. Ethyl acetate Salix alba leaves extract-loaded chitosan-based hydrogel film for wound dressing applications.

    PubMed

    Qureshi, Mohammad A; Khatoon, Fehmeeda; Rizvi, Moshahid A; Zafaryab, Md

    2015-01-01

    High toxicity and multidrug resistance associated with various standard antimicrobial drugs have necessitated search for safer alternatives in plant-derived materials. In this study, we performed biological examination of chitosan-based hydrogel film loaded with ethyl acetate Salix alba leaves extract against 11 standard laboratory strains. FTIR showed regeneration of saccharide peak in CP1A at 1047 cm(-1) and increased in height of other peaks. DSC exothermic decomposition peaks at 112 °C, 175 °C and 251 °C reveal the effect of extract on hydrogel film. From FESEM images, three-dimensional cross-linking and extract easily seen in the globular form from the surface. MTT assay on HEK 293 cells showed that CP1A was non-toxic. Minimum inhibitory concentration ranges from 4000 μg/ml to 125 μg/ml. Enterococcus faecium, Candida glabrata and Candida tropicalis were the most resistant, while Salmonella typhi and Candida guilliermondii were the most susceptible micro-organisms.

  15. Comparison of Kato-Katz, ethyl-acetate sedimentation, and Midi Parasep® in the diagnosis of hookworm, Ascaris and Trichuris infections in the context of an evaluation of rural sanitation in India.

    PubMed

    Funk, Anna L; Boisson, Sophie; Clasen, Thomas; Ensink, Jeroen H J

    2013-06-01

    The Kato-Katz, conventional ethyl-acetate sedimentation, and Midi Parasep(®) methods for diagnosing infection with soil-transmitted helminths were compared. The Kato-Katz technique gave the best overall diagnostic performance with the highest results in all measures (prevalence, faecal egg count, sensitivity) followed by the conventional ethyl-acetate and then the Midi Parasep(®) technique. The Kato-Katz technique showed a significantly higher faecal egg count and sensitivity for both hookworm and Trichuris as compared to the Midi Parasep(®) technique. The conventional ethyl-acetate technique produced smaller pellets and showed lower pellet mobility as compared to the Midi Parasep(®).

  16. Ethyl 2-(1,2,3,4-tetrahydro­spiro­[carba­zole-3,2′-[1,3]dioxolan]-9-yl)acetate

    PubMed Central

    Löffler, Philipp M. G.; Ulven, Trond; Bond, Andrew D.

    2009-01-01

    In the title compound, C18H21NO4, the hydrogenated six-membered ring of the carbazole unit adopts a half-chair conformation. The dioxolane ring and ethyl­acetate substituent point to opposite sides of the carbazole plane. The ethyl­acetate substituent adopts an essentially fully extended conformation, and its mean plane forms a dihedral angle of 83.8 (1)° with respect to the carbazole mean plane. The mol­ecules are arranged into stacks in which the carbazole planes form a dihedral angle of 4.4 (1)° and have an approximate inter­planar separation of 3.6 Å. PMID:21582427

  17. Validation and uncertainty analysis of a multi-residue method for pesticides in grapes using ethyl acetate extraction and liquid chromatography-tandem mass spectrometry.

    PubMed

    Banerjee, Kaushik; Oulkar, Dasharath P; Dasgupta, Soma; Patil, Shubhangi B; Patil, Sangram H; Savant, Rahul; Adsule, Pandurang G

    2007-11-30

    A method was validated for the multi-residue analysis of 82 pesticides in grapes at ethyl acetate (10 mL); cleaned by dispersive solid phase extraction and the results were obtained by liquid chromatography-tandem mass spectrometry. Reduction in sample size and proportion of ethyl acetate for extraction did not affect accuracy or precision of analysis when compared to the reported methods and was also statistically similar to the QuEChERS technique. The method was rugged (HorRat < 0.5) with <20% measurement uncertainties. Limit of quantification was <10 ng/g with recoveries 70-120% for most pesticides. The method offers cheaper and safer alternative to typical multi-residue analysis methods for grape.

  18. Evaluation of hydroxyapatite-bioglass and hydroxyapatite-ethyl vinyl acetate composite extracts on antioxidant defense mechanism and genotoxicity: an in vitro study.

    PubMed

    Arun, M; Silja, P K; Mohanan, P V

    2011-09-01

    Hydroxyapatite-bioglass (HA BG) and hydroxyapatite-ethyl vinyl acetate (HA EVA) are two composite materials that have been developed for bone substitution. Their activity on antioxidant defense mechanism and genotoxicity has not been investigated before. To further confirm its biocompatibility, the present study was undertaken to investigate the effect of HA BG and HA EVA on mice liver antioxidant mechanism along with chromosomal aberrations in human lymphocytes. Physiological saline extract of HA BG and HA EVA showed no adverse effect on liver antioxidant mechanism compared to the cyclophosphamide (CP)-induced toxicity on mice liver homogenate. The results were judged from the in vitro studies made on reduced glutathione, glutathione reductase and lipid peroxidation. These results were well supported by CP- and mytomycin C (MC)-induced genotoxicity studies on human lymphocytes in the presence and absence of a metabolic activator (S9). Hence, it was suggested that these tests could be considered for preliminary toxicological screening of materials intended for clinical applications ahead of in vivo animal model evaluation.

  19. Modification and re-validation of the ethyl acetate-based multi-residue method for pesticides in produce

    PubMed Central

    Rooseboom, Astrid; van Dam, Ruud; Roding, Marleen; Arondeus, Karin; Sunarto, Suryati

    2007-01-01

    The ethyl acetate-based multi-residue method for determination of pesticide residues in produce has been modified for gas chromatographic (GC) analysis by implementation of dispersive solid-phase extraction (using primary–secondary amine and graphitized carbon black) and large-volume (20 μL) injection. The same extract, before clean-up and after a change of solvent, was also analyzed by liquid chromatography with tandem mass spectrometry (LC–MS–MS). All aspects related to sample preparation were re-assessed with regard to ease and speed of the analysis. The principle of the extraction procedure (solvent, salt) was not changed, to avoid the possibility invalidating data acquired over past decades. The modifications were made with techniques currently commonly applied in routine laboratories, GC–MS and LC–MS–MS, in mind. The modified method enables processing (from homogenization until final extracts for both GC and LC) of 30 samples per eight hours per person. Limits of quantification (LOQs) of 0.01 mg kg−1 were achieved with both GC–MS (full-scan acquisition, 10 mg matrix equivalent injected) and LC–MS–MS (2 mg injected) for most of the pesticides. Validation data for 341 pesticides and degradation products are presented. A compilation of analytical quality-control data for pesticides routinely analyzed by GC–MS (135 compounds) and LC–MS–MS (136 compounds) in over 100 different matrices, obtained over a period of 15 months, are also presented and discussed. At the 0.05 mg kg−1 level acceptable recoveries were obtained for 93% (GC–MS) and 92% (LC–MS–MS) of pesticide–matrix combinations. PMID:17563885

  20. Genomic saturation mutagenesis and polygenic analysis identify novel yeast genes affecting ethyl acetate production, a non-selectable polygenic trait

    PubMed Central

    Abt, Tom Den; Souffriau, Ben; Foulquié-Moreno, Maria R.; Duitama, Jorge; Thevelein, Johan M.

    2016-01-01

    Isolation of mutants in populations of microorganisms has been a valuable tool in experimental genetics for decades. The main disadvantage, however, is the inability of isolating mutants in non-selectable polygenic traits. Most traits of organisms, however, are non-selectable and polygenic, including industrially important properties of microorganisms. The advent of powerful technologies for polygenic analysis of complex traits has allowed simultaneous identification of multiple causative mutations among many thousands of irrelevant mutations. We now show that this also applies to haploid strains of which the genome has been loaded with induced mutations so as to affect as many non-selectable, polygenic traits as possible. We have introduced about 900 mutations into single haploid yeast strains using multiple rounds of EMS mutagenesis, while maintaining the mating capacity required for genetic mapping. We screened the strains for defects in flavor production, an important non-selectable, polygenic trait in yeast alcoholic beverage production. A haploid strain with multiple induced mutations showing reduced ethyl acetate production in semi-anaerobic fermentation, was selected and the underlying quantitative trait loci (QTLs) were mapped using pooled-segregant whole-genome sequence analysis after crossing with an unrelated haploid strain. Reciprocal hemizygosity analysis and allele exchange identified PMA1 and CEM1 as causative mutant alleles and TPS1 as a causative genetic background allele. The case of CEM1 revealed that relevant mutations without observable effect in the haploid strain with multiple induced mutations (in this case due to defective mitochondria) can be identified by polygenic analysis as long as the mutations have an effect in part of the segregants (in this case those that regained fully functional mitochondria). Our results show that genomic saturation mutagenesis combined with complex trait polygenic analysis could be used successfully to

  1. Determination of amitraz and its transformation products in pears by ethyl acetate extraction and liquid chromatography-tandem mass spectrometry.

    PubMed

    Tokman, Nilgun; Soler, Carla; Farré, Marinel la; Picó, Yolanda; Barceló, Damià

    2009-04-10

    A method has been developed for identification and quantification of the acaricide amitraz and its transformation products, 2,4-dimethylaniline (DMA), 2,4-dimethylformamidine (DMF) and N-2,4-dimethylphenyl-N-methylformamidine (DMPF) in pears. The analytes were extracted using ethyl acetate and anhydrous sodium sulphate. Analysis was performed by liquid chromatography-electrospray tandem mass spectrometry (LC-ESI-MS/MS) in the positive ion mode using a triple quadrupole (QqQ) instrument. Two precursor-product ion transitions were monitored for each compound in the selected reaction monitoring (SRM) mode. The method was validated with pears taken from the orchard before the amitraz treatment and spiked at the limit of quantification (LOQ), 10 times the LOQ and the maximum residue limit (MRL). Recoveries were between 70 and 106% and relative standard deviations were below 19% (n=5 at each spiked level). Excellent sensitivity resulted in limits of detection (LODs) for all the compounds below 10 microg kg(-1). Quantification was carried out using matrix-matched standards calibration, response was a linear function of the concentration from the LOQs to, at least, three orders of magnitude. Recoveries and standard deviations were comparable to those obtained after hydrolysis of amitraz and its metabolites to DMA. Occurrence of amitraz and its metabolites in field-treated pears showed that, seven days after the treatment, DMPF and DMF are the main degradation products. This work reports for the first time the use of a conventional pesticide multiresidue method and LC-ESI-MS/MS for determining amitraz and its metabolites in pears.

  2. Different characteristic effects of ageing on starch-based films plasticised by 1-ethyl-3-methylimidazolium acetate and by glycerol.

    PubMed

    Zhang, Binjia; Xie, Fengwei; Zhang, Tianlong; Chen, Ling; Li, Xiaoxi; Truss, Rowan W; Halley, Peter J; Shamshina, Julia L; McNally, Tony; Rogers, Robin D

    2016-08-01

    The focus of this study was on the effects of plasticisers (the ionic liquid 1-ethyl-3-methylimidazolium acetate, or [Emim][OAc]; and glycerol) on the changes of starch structure on multiple length scales, and the variation in properties of plasticised starch-based films, during ageing. The films were prepared by a simple melt compression moulding process, followed by storage at different relative humidity (RH) environments. Compared with glycerol, [Emim][OAc] could result in greater homogeneity in [Emim][OAc]-plasticised starch-based films (no gel-like aggregates and less molecular order (crystallites) on the nano-scale). Besides, much weaker starch-starch interactions but stronger starch-[Emim][OAc] interactions at the molecular level led to reduced strength and stiffness but increased flexibility of the films. More importantly, [Emim][OAc] (especially at high content) was revealed to more effectively maintain the plasticised state during ageing than glycerol: the densification (especially in the amorphous regions) was suppressed; and the structural characteristics especially on the nano-scale were stabilised (especially at a high RH), presumably due to the suppressed starch molecular interactions by [Emim][OAc] as confirmed by Raman spectroscopy. Such behaviour contributed to stabilised mechanical properties. Nonetheless, the crystallinity and thermal stability of starch-based films with both plasticisers were much less affected by ageing and moisture uptake during storage (42 days), but mostly depended on the plasticiser type and content. As starch is a typical semi-crystalline bio-polymer containing abundant hydroxyl groups and strong hydrogen bonding, the findings here could also be significant in creating materials from other similar biopolymers with tailored sensitivity and properties to the environment.

  3. Genomic saturation mutagenesis and polygenic analysis identify novel yeast genes affecting ethyl acetate production, a non-selectable polygenic trait.

    PubMed

    Abt, Tom Den; Souffriau, Ben; Foulquié-Moreno, Maria R; Duitama, Jorge; Thevelein, Johan M

    2016-03-18

    Isolation of mutants in populations of microorganisms has been a valuable tool in experimental genetics for decades. The main disadvantage, however, is the inability of isolating mutants in non-selectable polygenic traits. Most traits of organisms, however, are non-selectable and polygenic, including industrially important properties of microorganisms. The advent of powerful technologies for polygenic analysis of complex traits has allowed simultaneous identification of multiple causative mutations among many thousands of irrelevant mutations. We now show that this also applies to haploid strains of which the genome has been loaded with induced mutations so as to affect as many non-selectable, polygenic traits as possible. We have introduced about 900 mutations into single haploid yeast strains using multiple rounds of EMS mutagenesis, while maintaining the mating capacity required for genetic mapping. We screened the strains for defects in flavor production, an important non-selectable, polygenic trait in yeast alcoholic beverage production. A haploid strain with multiple induced mutations showing reduced ethyl acetate production in semi-anaerobic fermentation, was selected and the underlying quantitative trait loci (QTLs) were mapped using pooled-segregant whole-genome sequence analysis after crossing with an unrelated haploid strain. Reciprocal hemizygosity analysis and allele exchange identified PMA1 and CEM1 as causative mutant alleles and TPS1 as a causative genetic background allele. The case of CEM1 revealed that relevant mutations without observable effect in the haploid strain with multiple induced mutations (in this case due to defective mitochondria) can be identified by polygenic analysis as long as the mutations have an effect in part of the segregants (in this case those that regained fully functional mitochondria). Our results show that genomic saturation mutagenesis combined with complex trait polygenic analysis could be used successfully to

  4. Ethyl Acetate Fraction of Amomum xanthioides Exerts Antihepatofibrotic Actions via the Regulation of Fibrogenic Cytokines in a Dimethylnitrosamine-Induced Rat Model

    PubMed Central

    Lee, Sung-Bae; Kim, Hyeong-Geug; Kim, Hyo-Seon; Lee, Jin-Seok; Im, Hwi-Jin; Kim, Won-Yong

    2016-01-01

    Amomum xanthioides has been traditionally used to treat diverse digestive system disorders in the Asian countries. We investigated antihepatofibrotic effects of ethyl acetate fraction of Amomum xanthioides (EFAX). Liver fibrosis is induced by dimethylnitrosamine (DMN) injection (intraperitoneally, 10 mg/kg of DMN for 4 weeks to Sprague-Dawley rats). EFAX (25 or 50 mg/kg), silymarin (50 mg/kg), or distilled water was orally administered every day. The DMN injection drastically altered body and organ mass, serum biochemistry, and platelet count, while EFAX treatment significantly attenuated this alteration. Severe liver fibrosis is determined by trichrome staining and measurement of hydroxyproline contents. EFAX treatment significantly attenuated these symptoms as well as the increase in oxidative by-products of lipid and protein metabolism in liver tissues. DMN induced a dramatic activation of hepatic stellate cells and increases in the levels of protein and gene expression of transforming growth factor-beta (TGF-β), platelet derived growth factor-beta (PDGF-β), and connective tissue growth factor (CTGF). Immunohistochemical analyses revealed increases in the levels of protein and gene expression of α-smooth muscle actin. These alterations were significantly normalized by EFAX treatment. Our findings demonstrate the potent antihepatofibrotic properties of EFAX via modulation of fibrogenic cytokines, especially TGF-β in the liver fibrosis rat model. PMID:27594891

  5. Antidepressant-like effects of the ethyl acetate soluble fraction of the root bark of Morus alba on the immobility behavior of rats in the forced swim test.

    PubMed

    Lim, Dong Wook; Kim, Yun Tai; Park, Ji-Hae; Baek, Nam-In; Han, Daeseok

    2014-06-12

    In this study, the antidepressant-like effects of Morus alba fractions in rats were investigated in the forced swim test (FST). Male Wistar rats (9-week-old) were administered orally the M. alba ethyl acetate (EtOAc 30 and 100 mg/kg) and M. alba n-butanol fractions (n-BuOH 30 and 100 mg/kg) every day for 7 consecutive days. On day 7, 1 h after the final administration of the fractions, the rats were exposed to the FST. M. alba EtOAc fraction at the dose of 100 mg/kg induced a decrease in immobility behavior (p < 0.01) with a concomitant increase in both climbing (p < 0.05) and swimming (p < 0.05) behaviors when compared with the control group, and M. alba EtOAc fraction at the dose of 100 mg/kg decreased the hypothalamic-pituitary-adrenal (HPA) axis response to the stress, as indicated by an attenuated corticosterone response and decreased c-fos immunoreactivity in the hippocampal and hypothalamic paraventricular nucleus (PVN) region. These findings demonstrated that M. alba EtOAc fraction have beneficial effects on depressive behaviors and restore both altered c-fos expression and HPA activity.

  6. Micelles Protect and Concentrate Activated Acetic Acid

    NASA Astrophysics Data System (ADS)

    Todd, Zoe; House, C.

    2014-01-01

    As more and more exoplanets are discovered and the habitability of such planets is considered, one can turn to searching for the origin of life on Earth in order to better understand what makes a habitable planet. Activated acetic acid, or methyl thioacetate, has been proposed to be central to the origin of life on Earth, and also as an important energy currency molecule in early cellular evolution. We have investigated the hydrolysis of methyl thioacetate under various conditions. Its uncatalyzed rate of hydrolysis is about three orders of magnitude faster (K = 0.00663 s^-1; 100°C, pH 7.5, concentration = 0.33mM) than published rates for its catalyzed production making it unlikely to accumulate under prebiotic conditions. However, we also observed that methyl thioacetate was protected from hydrolysis when inside its own hydrophobic droplets. We found that methyl thioacetate protection from hydrolysis was also possible in droplets of hexane and in the membranes of nonanoic acid micelles. Thus, the hydrophobic regions of prebiotic micelles and early cell membranes could have offered a refuge for this energetic molecule increasing its lifetime in close proximity to the reactions for which it would be needed. Methyl thioacetate could thus be important for the origin of life on Earth and perhaps for better understanding the potential habitability of other planets.

  7. Synthesis and Characterization of New Optically Active Poly (ethyl L-lysinamide)s and Poly (ethyl L-lysinimide)s

    PubMed Central

    Zahmatkesh, Saeed; Vakili, Mohammad Reza

    2010-01-01

    Ethyl L-lysine dihydrochloride was reacted with three different dianhydrides to yield the poly (ethyl L-lysinimide)s (PI1−3); it was also reacted with two different diacyl chlorides to yield the poly (ethyl L-lysinamide)s (PA4-5). The resulting polymers have inherent viscosities in the range of 0.15 to 0.42 dL g−1. These polymers are prepared from an inexpensive starting material and are optically active, potentially ion exchangeable, semicrystalline, thermally stable, and soluble in polar aprotic solvents such as DMF, DMSO, NMP, DMAc, and sulfuric acid. All of the above polymers were fully characterized by FT-IR and 1H NMR spectroscopy, elemental analysis, WAX diffraction, TGA, inherent viscosity measurement, and specific rotation. PMID:22331998

  8. Spectroscopic analysis (FT-IR, FT-Raman and NMR) and molecular docking study of ethyl 2-(4-oxo-3-phenethyl-3,4-dihydroquinazolin-2-ylthio)-acetate

    NASA Astrophysics Data System (ADS)

    El-Azab, Adel S.; Jalaja, K.; Abdel-Aziz, Alaa A.-M.; Al-Obaid, Abdulrahman M.; Sheena Mary, Y.; Yohannan Panicker, C.; Van Alsenoy, C.

    2016-09-01

    The vibrational wavenumbers, molecular structure, MEP, NLO, NBO and HOMO, LUMO analysis of Ethyl 2-(4-oxo-3-phenethyl-3,4-dihydroquinazolin-2-ylthio)-acetate (EPDA) were reported. The change in electron density in the antibonding orbitals and stabilization energies have been calculated by NBO analysis to give clear evidence of stabilization in the hyperconjugation of hydrogen bonded interaction. The difference in HOMO and LUMO energy support the charge transfer interaction within the molecule. NMR studies and Fukui functions are also reported. From molecular electrostatic potential plot it is evident that the negative charge covers the carbonyl groups, phenyl rings and the positive region is over the CH2 groups with the acetate group. Molecular docking studies shows that the title compound forms a stable complex with pyrrole inhibitor and gives a binding affinity value of -8.3 kcal/mol and the results suggest that the compound might exhibit inhibitory activity against pyrrole inhibitor.

  9. Synthesis and biological activity of thiazolyl-acetic acid derivatives as possible antimicrobial agents.

    PubMed

    Shirai, Akihiro; Fumoto, Yasuko; Shouno, Tomoaki; Maseda, Hideaki; Omasa, Takeshi

    2013-01-01

    5a-h, a series of (5-substituted-2-methyl-1,3-thiazole-4-yl) acetic acids as heterocyclic acetic acid derivatives, was designed and synthesized from ethyl acetoacetate. The synthesized compounds were screened for their antimicrobial activities against bacterial and fungal strains, and their characteristics were investigated by assays under various temperature and pH conditions. Cytotoxicity was evaluated with the use of sheep erythrocytes and human neonate dermal fibroblasts. Similarly, agents such as lauric acid 6 and parabens 7a-b, which are used as preservative agents for commercial cosmetics and detergents, were assayed for comparison. Although the structure of 5a is simple, comprising a thiazole attached with an octyl group and acetic acid moiety, the compound showed stronger and broader antibacterial and antifungal activities among the 5 series against the tested microbes other than gram-negative bacteria. Interestingly, 5a overcame the weak antifungal activity of parabens 7a-b. Also, the cytotoxicity of 5a was less than that of parabens 7a-b, especially to human dermal fibroblasts. These results suggest that thiazolyl-acetic acid 5a is a potentially effective biocide, and that it could be used as a preservative agent in commercially sold cosmetics and detergents, facilitated by the hydrophilic and charge properties of its carboxylic acid moiety.

  10. Effect of total hydroalcholic extract of Nigella sativa and its n-hexane and ethyl acetate fractions on ACHN and GP-293 cell lines.

    PubMed

    Shahraki, Samira; Khajavirad, Abolfazl; Shafei, Mohammad Naser; Mahmoudi, Mahmoud; Tabasi, Nafisa Sadat

    2016-01-01

    Medicinal plants are noted for their many advantages including the ability to treat diseases such as cancer. In this study, we examined the antitumor effect of the medicinal plant Nigella sativa on the morphology, survival, and apoptosis of ACHN (human renal adenocarcinoma) and GP-293 (normal renal epithelial) cell lines. From a hydroalcoholic extract of N. sativa, n-hexane and ethyl acetate fractions were extracted. Cells were treated with various concentrations of total hydroalcholic extract and n-hexane and ethyl acetate fractions; cell viability, morphological changes, and apoptosis were then determined. Results were presented as mean ± standard error of the mean (SEM). One-way analysis of variance (ANOVA) was applied for the statistical analysis of the data. The total extract and the fractions in a dose- and time-dependent manner reduced the cell viability in ACHN with no effect on the GP-293 cell line. In addition, the total extract resulted in more morphological changes in the ACHN cells compared to the GP-293 cells. The effect of the total extract in inducing apoptosis after 48 hours in the ACHN cell line was greater than in GP-293. In addition, the effect of the two fractions was lower than the total extract at all used concentrations. Therefore, the effect of total extract and n-hexane and ethyl acetate fractions of N. sativa on cell viability and apoptosis in the ACHN cell line is greater than in the GP-293 cell line. However, the effect of the total extract is higher than either of the two fractions on their own.

  11. Synergistic Anti-bacterial Effects of Phellinus baumii Ethyl Acetate Extracts and β-Lactam Antimicrobial Agents Against Methicillin-Resistant Staphylococcus aureus

    PubMed Central

    Hong, Seung Bok; Rhee, Man Hee; Yun, Bong-Sik; Lim, Young Hoon; Song, Hyung Geun

    2016-01-01

    Background The development of new drugs or alternative therapies effective against methicillin-resistant Staphylococcus aureus (MRSA) is of great importance, and various natural anti-MRSA products are good candidates for combination therapies. We evaluated the antibacterial activities of a Phellinus baumii ethyl acetate extract (PBEAE) and its synergistic effects with β-lactams against MRSA. Methods The broth microdilution method was used to determine the minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC) of the PBEAE. The PBEAE synergistic effects were determined by evaluating the MICs of anti-staphylococcal antibiotic mixtures, with or without PBEAE. Anti-MRSA synergistic bactericidal effects of the PBEAE and β-lactams were assessed by time-killing assay. An ELISA was used to determine the effect of the PBEAE on penicillin binding protein (PBP)2a production. Results The MICs and MBCs of PBEAE against MRSA were 256-512 and 1,024-2,048 µg/mL, respectively. The PBEAE significantly reduced MICs of all β-lactams tested, including oxacillin, cefazolin, cefepime, and penicillin. However, the PBEAE had little or no effect on the activity of non-β-lactams. Time-killing assays showed that the synergistic effects of two β-lactams (oxacillin and cefazolin) with the PBEAE were bactericidal in nature (Δlog10 colony forming unit/mL at 24 hr: 2.34-2.87 and 2.10-3.04, respectively). The PBEAE induced a dose-dependent decrease in PBP2a production by MRSA, suggesting that the inhibition of PBP2a production was a major synergistic mechanism between the β-lactams and the PBEAE. Conclusions PBEAE can enhance the efficacy of β-lactams for combined therapy in patients infected with MRSA. PMID:26709257

  12. Antimycobacterial activity of two natural alkaloids, vasicine acetate and 2-acetyl benzylamine, isolated from Indian shrub Adhatoda vasica Ness. leaves.

    PubMed

    Ignacimuthu, S; Shanmugam, N

    2010-12-01

    In folk medicine, Adhatoda vasica Ness. (Acanthaceae) is used to treat asthma and cough. The leaves of A. vasica were powdered and extracted with hexane, ethyl acetate and methanol. The hexane extract showed 97 percent reduction in colony-forming units (CFU) at 100 microg/ml. The hexane extract was subjected to column chromatography. Two natural compounds, vasicine acetate and 2-acetyl benzylamine, were isolated from it. They were bioassayed against Mycobacterium tuberculosis. The two compounds showed strong antimycobacterial activity. Vasicine acetate and 2-acetyl benzylamine isolated from hexane extract of A. vasica leaves, significantly inhibited M. tuberculosis and one multi-drug-resistant (MDR) strain and one sensitive strain at 200 and 50 microg/ml, respectively. Our study demonstrated that both the compounds, vasicine acetate and 2-acetyl benzylamine, could be evaluated further for developing a drug to control M. tuberculosis.

  13. Anti-inflammatory potential of an ethyl acetate fraction isolated from Justicia gendarussa roots through inhibition of iNOS and COX-2 expression via NF-κB pathway.

    PubMed

    Kumar, Kavitha S; Vijayan, Viji; Bhaskar, Shobha; Krishnan, Kripa; Shalini, V; Helen, A

    2012-01-01

    Justicia gendarussa Burm.f. (J. gendarussa) is a plant used as traditional medicine in different parts of India and China to treat inflammatory disorders like rheumatoid arthritis. But its mechanism of anti-inflammatory action is still unclear. Hence in this context, the objective of our study is to reveal the mechanism of anti-inflammatory activity of J. gendarussa which would form an additional proof to the traditional knowledge of this plant. The anti-inflammatory function and mechanism(s) of action was studied in an ethyl acetate fraction isolated from methanolic extract of J. gendarussa roots (EJG). Anti-inflammatory studies were conducted on rats using partitioned fractions isolated from methanolic extract of J. gendarussa roots. In carrageenan-induced rat paw edema, ethyl acetate fraction brought about 80% and 93% edema inhibition at 3rd and 5th hour at a dose of 50 mg/kg, when compared to other extracts and Voveran. We investigated whether EJG inhibits the release of cycloxygenase (COX), 5-lipoxygenase (5-LOX), interleukin-6 (IL-6) and nuclear factor kappa B (NF-κB) in LPS stimulated human peripheral blood mononuclear cells (hPBMCs). Results shows that EJG dose dependently inhibited LPS-activated COX, 5-LOX, IL-6, and NF-κB in hPBMCs. EJG also reduced LPS induced levels of iNOS and COX-2 mRNA expression in hPBMCs. This study provides an insight into the probable mechanism(s) underlying the anti-inflammatory activity of EJG and therefore, we report the first confirmation of the anti-inflammatory potential of this traditionally employed herbal medicine in vitro.

  14. Mixture Toxicity of SN2-Reactive Soft Electrophiles: 3. Evaluation of Ethyl α-Halogenated Acetates with α-Halogenated Acetonitriles

    PubMed Central

    Pöch, G.; Schultz, T. W.

    2014-01-01

    Mixture toxicity for each of four ethyl α-halogenated acetates (ExACs) with each of three α-halogenated acetonitriles (xANs) was assessed. Inhibition of bioluminescence in Vibrio fischeri was measured after 15, 30 and 45-min of exposure. Concentration-response curves were developed for each chemical at each exposure duration and used to develop predicted concentration-response curves for the dose-addition and independence models of combined effect. Concentration-response curves for each mixture and each exposure duration were then evaluated against the predicted curves, using three metrics per model: 1) EC50-based additivity quotient (AQ) or independence quotient (IQ) values, 2) mean AQ (mAQ) or mean IQ (mIQ) values, calculated by averaging the EC25, EC50 and EC75 AQ or IQ values, and 3) deviation values from additivity (DV-A) or independence (DV-I). Mixture toxicity for ethyl iodoacetate (EIAC) was dose-additive with each of the xANs at all exposure durations and was often consistent with independence as well. The same was true for mixture toxicity of ethyl bromoacetate (EBAC) with each xAN. However, for the two more slowly reactive chemicals ethyl chloroacetate (ECAC) and ethyl fluoroacetate (EFAC) mixture toxicity with each xAN only became consistent with dose-addition upon increasing exposure duration. Consistency with independence for both ECAC and EFAC with the xANs was essentially limited to the EC50-IQ metric; thereby demonstrating the utility of calculating the mean quotient (mAQ, mIQ) and deviation value (DV-A, DV-I) metrics. Upon review of these findings with those from the first two papers in the series, the results suggest that instances in which mixture toxicity was not consistent with dose-addition relate: 1) to differences in the capability of the chemicals to form strong H-bonds with water and 2) to differences in relative reactivity and time-dependent toxicity levels of the chemicals. PMID:24368709

  15. Sulfur Ylides. Communication 1. Cyclopropanation of. cap alpha. ,. beta. -unsaturated Ketones with Ethyl (dimethylsulfuranylidene) acetate generated in the presence of phase-transfer catalysts

    SciTech Connect

    Tolstikov, G.A.; Galin, F.Z.; Iskandarova V.N.; Khalilov, L.M.; Panasenko, A.A.

    1986-04-01

    This paper presents a modified method for the cyclopropanation of alpha, beta-unsaturated ketones with ethyl (dimethylsulfuranylidene) acetate, generated in situ from a sulfonium salt with 85% KOH in the presence of a phase-transfer catalyst, and studies the sterochemistry of the polysubstituted cyclopropanes. The chemical shifts of the carbon atoms of the cyclopropane rings of the isomer pairs are close together in the C 13 NMR spectra, which makes the assignment of the signals of C/sup 2/ and C/sup 3/ and the sterochemical assignment of each isomer to the cis and the trans series difficult. It is shown that the signals of the carboxyl carbon atoms differ not more than 0.65 ppm in the isomer pairs.

  16. Characteristics of lipid extraction from Chlorella sp. cultivated in outdoor raceway ponds with mixture of ethyl acetate and ethanol for biodiesel production.

    PubMed

    Lu, Weidong; Wang, Zhongming; Yuan, Zhenhong

    2015-09-01

    In this work, neutral lipids (NLs) extraction capacity and selectivity of six solvents were firstly compared. In addition, an eco-friendly solvent combination of ethyl acetate and ethanol (EA/E) was proposed and tested for lipid extraction from Chlorella sp. cultivated in outdoor raceway ponds and effect of extraction variables on lipid yield were intensively studied. Results indicated that lipid extraction yield was increased with solvent to biomass ratio but did not vary significantly when the value exceeded 20:1. Lipid yield was found to be strongly dependent on extraction temperature and time. Finally, fatty acid profiles of lipid were determined and results indicated that the major components were octadecanoic acid, palmitic acid, linoleic acid and linolenic acid, demonstrating that the lipid extracted from the Chlorella sp. cultivated in outdoor raceway ponds by EA/E was suitable feedstock for biodiesel production.

  17. Galangal pungent component, 1'-acetoxychavicol acetate, activates TRPA1.

    PubMed

    Narukawa, Masataka; Koizumi, Kanako; Iwasaki, Yusaku; Kubota, Kikue; Watanabe, Tatsuo

    2010-01-01

    We investigated the activation of transient receptor potential cation channel (TRP) subfamily V, member 1 (TRPV1) and TRP subfamily A, member 1 (TRPA1) by 1'-acetoxychavicol acetate (ACA), the main pungent component in galangal. ACA did not activate TRPV1-expressing human embryonic kidney (HEK) cells, but strongly activated TRPA1-expressing HEK cells. ACA was more potent than allyl isothiocyanate, the typical TRPA1 agonist.

  18. Higher hypochlorous acid scavenging activity of ethyl pyruvate compared to its sodium salt.

    PubMed

    Olek, Robert Antoni; Ziolkowski, Wieslaw; Kaczor, Jan Jacek; Wierzba, Tomasz Henryk; Antosiewicz, Jedrzej

    2011-01-01

    Although a number of studies have focused on the higher ethyl pyruvate antioxidative activity than its sodium salt under various stress conditions, and the greater protective properties of the ester form have been suggested as the effect of better cell membrane penetration, the molecular mechanism has remained unclear. The aim of the present study was therefore to compare the antioxidative activities of sodium and ethyl pyruvate under in vitro conditions by using a liver homogenate as the model for cell membrane transport deletion. The potential effect of ethanol was also evaluated, and hypochlorous acid was used as an oxidant. Our data indicate the concentration-dependent scavenging potency of both sodium and ethyl pyruvate, with the ester having higher activity. This effect was not related to the presence of ethanol. Better protection of the liver homogenate by ethyl pyruvate was also apparent, despite the fact that cell membrane transport was omitted.

  19. 40 CFR 180.595 - Flufenpyr-ethyl; tolerances for residues.

    Code of Federal Regulations, 2014 CFR

    2014-07-01

    ... residues of the herbicide, flufenpyr-ethyl; acetic acid, -phenoxy]-ethyl ester], in or on the following...) Tolerances are established for residues of the herbicide flufenpyr-ethyl; acetic acid, -phenoxy]-ethyl...

  20. 40 CFR 180.595 - Flufenpyr-ethyl; tolerances for residues.

    Code of Federal Regulations, 2010 CFR

    2010-07-01

    ... residues of the herbicide, flufenpyr-ethyl; acetic acid, -phenoxy]-ethyl ester], in or on the following...) Tolerances are established for residues of the herbicide flufenpyr-ethyl; acetic acid, -phenoxy]-ethyl...

  1. 40 CFR 180.595 - Flufenpyr-ethyl; tolerances for residues.

    Code of Federal Regulations, 2013 CFR

    2013-07-01

    ... residues of the herbicide, flufenpyr-ethyl; acetic acid, -phenoxy]-ethyl ester], in or on the following...) Tolerances are established for residues of the herbicide flufenpyr-ethyl; acetic acid, -phenoxy]-ethyl...

  2. 40 CFR 180.595 - Flufenpyr-ethyl; tolerances for residues.

    Code of Federal Regulations, 2011 CFR

    2011-07-01

    ... residues of the herbicide, flufenpyr-ethyl; acetic acid, -phenoxy]-ethyl ester], in or on the following...) Tolerances are established for residues of the herbicide flufenpyr-ethyl; acetic acid, -phenoxy]-ethyl...

  3. 40 CFR 180.595 - Flufenpyr-ethyl; tolerances for residues.

    Code of Federal Regulations, 2012 CFR

    2012-07-01

    ... residues of the herbicide, flufenpyr-ethyl; acetic acid, -phenoxy]-ethyl ester], in or on the following...) Tolerances are established for residues of the herbicide flufenpyr-ethyl; acetic acid, -phenoxy]-ethyl...

  4. 21 CFR 184.1295 - Ethyl formate.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... Substances Affirmed as GRAS § 184.1295 Ethyl formate. (a) Ethyl formate (C3H6O2, CAS Reg. No. 109-94-4) is also referred to as ethyl methanoate. It is an ester of formic acid and is prepared by esterification of formic acid with ethyl alcohol or by distillation of ethyl acetate and formic acid in the...

  5. 21 CFR 184.1295 - Ethyl formate.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... Substances Affirmed as GRAS § 184.1295 Ethyl formate. (a) Ethyl formate (C3H6O2, CAS Reg. No. 109-94-4) is also referred to as ethyl methanoate. It is an ester of formic acid and is prepared by esterification of formic acid with ethyl alcohol or by distillation of ethyl acetate and formic acid in the...

  6. Synthesis and herbicidal activities of benzothiazole N,O-acetals.

    PubMed

    Ji, Zhiqin; Zhou, Fengxing; Wei, Shaopeng

    2015-10-01

    A new series of N,O-acetals were prepared via a simple one-pot reaction by the condensation of 2-amino-methybenzothiazole with aldehydes and alcohols. The title compounds were obtained in moderate to good yields in the presence of acid catalyst. Bioassay results indicated that some synthesized compounds had good herbicidal activity against both dicotyledon and monocotyledon weeds. This investigation provided a new type of herbicidal lead compounds, as well as its facile preparation method.

  7. Effect of vanillin and ethyl vanillin on cytochrome P450 activity in vitro and in vivo.

    PubMed

    Chen, Xiao-min; Wei, Min; Zhang, Hai-mou; Luo, Cheng-hao; Chen, Yi-kun; Chen, Yong

    2012-06-01

    Food safety is of extreme importance to human health. Vanillin and ethyl vanillin are the widely used food additives and spices in foods, beverages, cosmetics and drugs. The objective of the present work was to evaluate the impact of vanillin and ethyl vanillin on the activities of CYP2C9, CYP2E1, CYP3A4, CYP2B6 and CYP1A2 in human liver microsomes (HLM) in vitro, and impact on the activities of CYP1A2, CYP2C, CYP3A and CYP2E1 in rat liver microsomes (RLM) in vivo. The in vitro results demonstrated that vanillin and ethyl vanillin had no significant effect on the activity of five human CYP450 enzymes with concentration ranged from 8 to 128 μM. However, after rats were orally administered vanillin or ethyl vanillin once a day for seven consecutive days, CYP2E1 activity was increased and CYP1A2 activity was decreased in RLM. The in vivo results revealed that drug interaction between vanillin/ethyl vanillin and the CYP2E1/CYP1A2-metabolizing drugs might be possible, and also suggested that the application of the above additives in foods and drugs should not be unlimited so as to avoid the adverse interaction.

  8. In situ morphological assessment of apoptosis induced by Phaleria macrocarpa (Boerl.) fruit ethyl acetate fraction (PMEAF) in MDA-MB-231 cells by microscopy observation.

    PubMed

    Kavitha, Nowroji; Chen, Yeng; Kanwar, Jagat R; Sasidharan, Sreenivasan

    2017-03-01

    Phaleria macrocarpa (Boerl.) is a well-known medicinal plant and have been extensively used as traditional medicine for ages in treatment of various diseases. The purpose of this study was to determine the in situ cytotoxicity effect P. macrocarpa fruit ethyl acetate fraction (PMEAF) by using various conventional and modern microscopy techniques. The cytotoxicity of PMEAF treated MDA-MB-231 cells was determined through the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) cytotoxicity assay and CyQuant Cell Proliferation Assay after 24h of treatment. Both results were indicated that the PMEAF is a potential anticancer agent with the average IC50 values of 18.10μg/mL by inhibiting the MDA-MB-231 cell proliferation. Various conventional and modern microscopy techniques such as light microscopy, holographic microscopy, transmission (TEM) and scanning (SEM) electron microscope were used for the observation of morphological changes in PMEAF treated MDA-MB-231cells for 24h. The characteristic of apoptotic cell death includes cell shrinkage, membrane blebs, chromatin condensation and the formation of apoptotic bodies were observed. PMEAF might be the best candidate for developing more potent anticancer drugs or chemo-preventive supplements.

  9. Chemical fingerprint and metabolic profile analysis of ethyl acetate fraction of Gastrodia elata by ultra performance liquid chromatography/quadrupole-time of flight mass spectrometry.

    PubMed

    Tang, Chunlan; Wang, Li; Liu, Xinxin; Cheng, Mengchun; Xiao, Hongbin

    2016-02-01

    The chemical fingerprint and metabolic profile of traditional Chinese medicine is very complicated and has been a great challenge. In the present study, chemical fingerprint of ethyl acetate fraction of Gastrodia elata (EtAcGE) and metabolic profile of rat plasma sample after intragastric administration of EtAcGE (2.5g/kg) were investigated using ultra-high performance liquid chromatography coupled with quadrupole-time of flight mass spectrometry (UPLC/Q-TOF MS). A total of 38 chemical constituents of EtAcGE were identified by comparing their retention time, accurate molecular mass and characteristic fragment ions with those of references, or tentatively characterized by comparing molecular formula, fragment ions with that of known compound or information available in literature. And 40 compounds were detected in dosed rat plasma sample, including 16 prototypes and 24 metabolites underwent metabolic process of glucuronidation, glucosylation, sulfation, methylation, hydroxylation, dehydrogenation or mixed modes. The metabolic "soft spots" was hydroxyl or carboxy group. This is the first research for chemical fingerprint and metabolic profile of EtAcGE, which lay a foundation for the further investigation of EtAcGE.

  10. Comparative evaluation of the metabolic effects of hydroxytyrosol and its lipophilic derivatives (hydroxytyrosyl acetate and ethyl hydroxytyrosyl ether) in hypercholesterolemic rats.

    PubMed

    Tabernero, María; Sarriá, Beatriz; Largo, Carlota; Martínez-López, Sara; Madrona, Andrés; Espartero, José Luis; Bravo, Laura; Mateos, Raquel

    2014-07-25

    Hydroxytyrosol (HT), a virgin olive oil phenolic phytochemical with proven health benefits, has been used to generate new lipophilic antioxidants to preserve fats and oils against autoxidation. The aim of this work is to comparatively evaluate the physiological effects of HT and its lipophilic derivatives, hydroxytyrosyl acetate (HT-Ac) and ethyl hydroxytyrosyl ether (HT-Et), in high-cholesterol fed animals. Male Wistar rats (n = 8) were fed a standard diet (C group), a cholesterol-rich diet (Chol group) or a cholesterol-rich diet supplemented with phenolic compounds (HT group, HT-Ac group and HT-Et group) for 8 weeks. Body and tissue weights, the lipid profile, redox status, and biochemical, hormonal, and inflammatory biomarkers were evaluated. Plasma levels of total cholesterol, LDL cholesterol, glucose, insulin and leptin, as well as malondialdehyde in serum increased in Chol compared to C (p < 0.05). Rats fed the test diets had improved glucose, insulin, leptin and MDA levels and antioxidant capacity status, with HT-Ac being the most effective compound. The studied phenolic compounds also modulated TNF-α and IL-1β plasma levels compared to Chol. HT-Ac and HT-Et improved adipose tissue distribution and adipokine production, decreasing MCP-1 and IL-1β levels. Our results confirm the metabolic effects of HT, which are maintained and even improved by hydrophobic derivatives, particularly HT-Ac.

  11. Characteristics of starch-based films plasticised by glycerol and by the ionic liquid 1-ethyl-3-methylimidazolium acetate: a comparative study.

    PubMed

    Xie, Fengwei; Flanagan, Bernadine M; Li, Ming; Sangwan, Parveen; Truss, Rowan W; Halley, Peter J; Strounina, Ekaterina V; Whittaker, Andrew K; Gidley, Michael J; Dean, Katherine M; Shamshina, Julia L; Rogers, Robin D; McNally, Tony

    2014-10-13

    This paper reports the plasticisation effect of the ionic liquid, 1-ethyl-3-methylimidazolium acetate ([Emim][OAc]), as compared with the traditionally used plasticiser, glycerol, on the characteristics of starch-based films. For minimising the additional effect of processing, a simple compression moulding process (which involves minimal shear) was used for preparation of starch-based films. The results show that [Emim][OAc] was favourable for plasticisation, i.e., disruption of starch granules (by scanning electron microscopy), and could result in a more amorphous structure in the starch-based materials (by X-ray diffraction and dynamic mechanical analysis). (13)C CP/MAS and SPE/MAS NMR spectroscopy revealed that not only was the crystallinity reduced by [Emim][OAc], but also the amorphous starch present was plasticised to a more mobile form as indicated by the appearance of amorphous starch in the SPE/MAS spectrum. Mechanical results illustrate that, when either glycerol or [Emim][OAc] was used, a higher plasticiser content could contribute to higher flexibility. In spite of the accelerated thermal degradation of starch by [Emim][OAc] as shown by thermogravimetric analysis, the biodegradation study revealed the antimicrobial effect of [Emim][OAc] on the starch-based materials. Considering the high-amylose starch used here which is typically difficult to gelatinise in a traditional plasticiser (water and/or glycerol), [Emim][OAc] is demonstrated to be a promising plasticiser for starch to develop "green" flexible antimicrobial materials for novel applications.

  12. Pre-dispersed organo-montmorillonite (organo-MMT) nanofiller: Morphology, cytocompatibility and impact on flexibility, toughness and biostability of biomedical ethyl vinyl acetate (EVA) copolymer.

    PubMed

    Osman, Azlin F; M Fitri, Tuty Fareyhynn; Rakibuddin, Md; Hashim, Fatimah; Tuan Johari, Syed Ahmad Tajudin; Ananthakrishnan, Rajakumar; Ramli, Rafiza

    2017-05-01

    Polymer-clay based nanocomposites are among the attractive materials to be applied for various applications, including biomedical. The incorporation of the nano sized clay (nanoclay) into polymer matrices can result in their remarkable improvement in mechanical, thermal and barrier properties as long as the nanofillers are well exfoliated and dispersed throughout the matrix. In this work, exfoliation strategy through pre-dispersing process of the organically modified montmorillonite (organo-MMT) nanofiller was done to obtain ethyl vinyl acetate (EVA) nanocomposite with improved flexibility, toughness, thermal stability and biostability. Our results indicated that the degree of organo-MMT exfoliation affects its cytotoxicity level and the properties of the resulting EVA nanocomposite. The pre-dispersed organo-MMT by ultrasonication in water possesses higher degree of exfoliation as compared to its origin condition and significantly performed reduced cytotoxicity level. Beneficially, this nanofiller also enhanced the EVA flexibility, thermal stability and biostability upon the in vitro exposure. We postulated that these were due to plasticizing effect and enhanced EVA-nanofiller interactions contributing to more stable chemical bonds in the main copolymer chains. Improvement in copolymer flexibility is beneficial for close contact with human soft tissue, while enhancement in toughness and biostability is crucial to extend its life expectancy as insulation material for implantable device.

  13. Development of Paper, Chemical Agent Detector, 3-Way Liquid Containing Non-Mutagenic Dyes. 2. Replacement of the Blue Indicator Dye Ethyl-bis-(2,4- Dinitrophenyl Acetate (EDA)

    DTIC Science & Technology

    1988-06-01

    OL JU)OY (ý2ýPj 00 (V)~ Oetence nationale DTI DEVELOPIIEnT OF PAPER, CHEMICAL AGENT DETECTOR, 3-WAY LIQUID CONTAINING NON-MUTAGENIC DYES . Hi...REPLACEMENT OF THE BLUE INflICATOR DYE ETH.YL-b is-(2.4-DI NITROPH ENYL) ACETATE IEDA) by D. Thoravala, J.W. Bovenkampb, R.W. Betsa and B.V. Lcroixb...NON-MUTAGENIC DYES . n-REPLACEMENT OF THE BLUE INDICATOR DYE ETHYL-bis-(2,4-DINITROPHENYL) ACETATE (EDA) by D. Thoraval and R.W. Bets Anachemic Canada

  14. Antiangiogenic Activity of Glycyrrhiza Extract

    NASA Astrophysics Data System (ADS)

    Li, Ying-Qiu

    The bioactivity of extract of glycyrrhiza was detected by zebrafish antiangiogenic model after 70% ethanol extract of glycyrrhiza was extracted with petroleum ether, ethyl acetate, n-butanol. The inhibition of the extracts in antiangiogenic activity showed that the highest active components existed in ethyl acetate extract of glycyrrhiza. The ethyl acetate extract of glycyrrhiza was separated by polyamide column chromatography to obtain 7 fractions (Fr1-Fr7), which Fr5 and Fr6 showed antiangiogenic activity.

  15. Ethyl acetate fraction of adlay bran ethanolic extract inhibits oncogene expression and suppresses DMH-induced preneoplastic lesions of the colon in F344 rats through an anti-inflammatory pathway.

    PubMed

    Chung, Cheng-Pei; Hsu, Hsin-Yi; Huang, Din-Wen; Hsu, Hsing-Hua; Lin, Ju-Tsui; Shih, Chun-Kuang; Chiang, Wenchang

    2010-07-14

    Adlay ( Coix lachryma-jobi L. var. ma-yuen Stapf) is a grass crop and was reported to possess anti-inflammatory activity and an antiproliferative effect in cancer cell lines. The purpose of this study was to evaluate the effects of the ethyl acetate fraction of an adlay bran ethanolic extract (ABE-Ea) on colon carcinogenesis in an animal model and investigate its mechanism. Male F344 rats received 1,2-dimethylhydrazine (DMH) and consumed different doses of ABE-Ea. The medium-dose group (17.28 mg of ABE-Ea/day) exhibited the best suppressive effect on colon carcinogenesis and prevented preneoplastic mucin-depleted foci (MDF) formation. Moreover, RAS and Ets2 oncogenes were significantly down-regulated in this group compared to the negative control group, whereas Wee1, a gene involved in the cell cycle, was up-regulated. Cyclooxygenase-2 (COX-2) protein expression was significantly suppressed in all colons receiving the ABE-Ea, indicating that ABE-Ea delayed carcinogenesis by suppressing chronic inflammation. ABE-Ea included considerable a proportion of phenolic compounds, and ferulic acid was the major phenolic acid (5206 microg/g ABE-Ea) on the basis of HPLC analysis. Results from this study suggest that ABE-Ea suppressed DMH-indued preneoplastic lesions of the colon in F344 rats and that ferulic acid may be one of the active compounds.

  16. Aerobic biotransformation and fate of N-ethyl perfluorooctane sulfonamidoethanol (N-EtFOSE) in activated sludge.

    PubMed

    Rhoads, Kurt R; Janssen, Elisabeth M L; Luthy, Richard G; Criddle, Craig S

    2008-04-15

    Processes affecting the fate of perfluorinated organics are of increasing concern due to the global dispersal, persistence, and bioaccumulation of these contaminants. The volatile compound N-ethyl perfluorooctane sulfonamidoethanol (N-EtFOSE) and its phosphate esters have been used in protective surface coatings. In this report, we describe the fate of N-EtFOSE in aerobic batch assays. These assays were performed using undiluted activated sludge in serum bottles that were sealed to prevent the escape of N-EtFOSE and volatile transformation products. Separate assays were performed with N-EtFOSE and reported transformation products. N-EtFOSE degraded to N-ethyl perfluorooctane sulfonamido acetic acid (N-EtFOSAA) with an observed first-order rate of 0.99 +/- 0.08 day(-1) and a pseudosecond order rate of 0.26 +/- 0.02 L/mg VSS day(-1). N-EtFOSAA underwent further transformation at a slower rate (0.093 +/- 0.012 day(-1)) to N-ethylperfluorooctane sulfonamide (N-EtFOSA). N-EtFOSA then transformed to perfluorooctane sulfonamide (FOSA). FOSA transformed to perfluorooctane sulfinate (PFOSI), and PFOSI transformed to perfluorooctane sulfonate (PFOS). Perfluorooctanoic acid (PFOA) was not detected as a transformation product of any compound. Using the measured rate of N-EtFOSE biotransformation and literature values for phase partitioning and mass transfer in aeration basins, we modeled the fate of N-EtFOSE in a typical activated sludge aeration basin open to the atmosphere. The model predicts that 76% of the N-EtFOSE is stripped into the atmosphere, 5% sorbs to waste solids, 13% undergoes transformation to N-EtFOSAA, and 6% is discharged in the wastewater effluent.

  17. Crystal structure of ethyl 2-[9-(5-bromo-2-hy-droxy-phen-yl)-1,8-dioxo-1,2,3,4,5,6,7,8,9,10-deca-hydro-acridin-10-yl]acetate.

    PubMed

    Mohamed, Shaaban K; Akkurt, Mehmet; Jasinski, Jerry P; Abdelhamid, Antar A; Tamam, Asmaa H; Albayati, Mustafa R

    2015-12-01

    In the title compound, C23H24BrNO5, the central 1,4-di-hydro-pyridine ring of the 1,2,3,4,5,6,7,8,9,10-deca-hydro-acridine ring system adopts a half-chair conformation. The two cyclo-hexene rings fused to the central ring both have a twisted-boat conformation. The mean planes of the bromo-hydroxy-phenyl ring and the major and minor components of the disordered ethyl amino-acetate moiety make dihedral angles of 78.99 (12), 85.9 (2) and 88.3 (9)°, respectively, with the 1,4-di-hydro-pyridine ring. The terminal ethyl group of the ethyl amino-acetate moiety is disordered over two sets of sites with refined occupancies of 0.768 (17) and 0.232 (17). The mol-ecular conformation is stabilized by an intra-molecular O-H⋯O hydrogen bond, forming an S(8) ring motif. In the crystal, C-H⋯O hydrogen bonds connect the mol-ecules into layers parallel to (001), enclosing R 1 (2)(7) ring motifs.

  18. In vitro antitumor activity of the ethyl acetate extract of Potentilla chinensis in osteosarcoma cancer cells

    PubMed Central

    Wan, Guang; Tao, Jin-Gang; Wang, Guo-Dong; Liu, Shen-Peng; Zhao, Hong-Xing; Liang, Qiu-Dong

    2016-01-01

    The aim of the current study was to evaluate the anticancer effect of the ethanol extract of Potentilla chinensis, a Chinese medicinal plant. An MTT assay was used to evaluate the cell viability of MG-63 human osteosarcoma cancer cells and fR-2 cells. Furthermore, the effect of the extract on apoptosis induction, cell cycle phase distribution and inhibition of cell migration in the MG63 human osteosarcoma cancer cell line was evaluated. The effect of the extract on cell cycle phase distribution was assessed by flow cytometry using propidium iodide (PI). Phase contrast microscopy detected the morphological changes in MG63 cancer cells following extract treatment. The results of the study demonstrated that the extract was cytotoxic to MG63 cancer cells, while the normal cell line (epithelial cell line) showed lower susceptibility. Phase contrast microscopy showed distinguishing morphological features, such as cell shrinkage and blebbing induced by the extract treatment in osteosarcoma cancer cells. The average proportion of Annexin V-positive cells (total apoptotic cells) significantly increased from 5.6% in the control to 24.2, 38.8 and 55.7% in the 40, 80 and 150 µg/ml groups, respectively. The extract induced early and late apoptosis in the cancer cells. Flow cytometric analysis revealed that the extract induced G0/G1-cell cycle arrest, which also showed significant dose-dependence. The extract induced a significant and concentration-dependent reduction in cell migration. Moreover, DNA fragmentation was also examined by observation of the formation of DNA ladders. It was demonstrated that DNA fragmentation was increased with extract concentration compared with that in the control. Taken together, EEPC may serve as potential therapeutic agent against osteosarcoma, provided that the toxicity profile and in vivo investigations demonstrate that it is safe. PMID:27573158

  19. Anti-wrinkle effects of Sargassum muticum ethyl acetate fraction on ultraviolet B-irradiated hairless mouse skin and mechanistic evaluation in the human HaCaT keratinocyte cell line

    PubMed Central

    Song, Jae Hyoung; Piao, Mei Jing; Han, Xia; Kang, Kyoung Ah; Kang, Hee Kyoung; Yoon, Weon Jong; Ko, Mi Hee; Lee, Nam Ho; Lee, Mi Young; Chae, Sungwook; Hyun, Jin Won

    2016-01-01

    The present study investigated the photoprotective properties of the ethyl acetate fraction of Sargassum muticum (SME) against ultraviolet B (UVB)-induced skin damage and photoaging in a mouse model. HR-1 strain hairless male mice were divided into three groups: An untreated control group, a UVB-irradiated vehicle group and a UVB-irradiated SME group. The UVB-irradiated mice in the SME group were orally administered with SME (100 mg/kg body weight in 0.1 ml water per day) and then exposed to radiation at a dose of 60–120 mJ/cm2. Wrinkle formation and skin damage were evaluated by analysis of skin replicas, epidermal thickness and collagen fiber integrity in the dermal connective tissue. The mechanism underlying the action of SME was also investigated in the human HaCaT keratinocyte cell line following exposure of the cells to UVB at a dose of 30 mJ/cm2. The protein expression levels and activity of matrix metalloproteinase-1 (MMP-1), and the binding of activator protein-1 (AP-1) to the MMP-1 promoter were assessed in the HaCaT cells using western blot analysis, an MMP-1 fluorescent assay and a chromatin immune-precipitation assay, respectively. The results showed that the mean length and depth of the wrinkles in the UVB-exposed hairless mice were significantly improved by oral administration of SME, which also prevented the increase in epidermal thickness triggered by UVB irradiation. Furthermore, a marked increase in collagen bundle formation was observed in the UVB-treated mice with SME administration. SME pretreatment also significantly inhibited the UVB-induced upregulation in the expression and activity of MMP-1 in the cultured HaCaT keratinocytes, and the UVB-enhanced association of AP-1 with the MMP-1 promoter. These results suggested that SME may be useful as an anti-photoaging resource for the skin. PMID:27573915

  20. Synthesis and antitumor activity of new amphiphilic alkylglycerolipids substituted with a polar head group, 2-(2-trimethylammonioethoxy)ethyl or a congeneric oligo(ethyleneoxy)ethyl group.

    PubMed

    Ukawa, K; Imamiya, E; Yamamoto, H; Aono, T; Kozai, Y; Okutani, T; Nomura, H; Honma, Y; Hozumi, M; Kudo, I

    1989-12-01

    A new series of amphiphilic 1-octadecyl glycerolipids (eleven compounds, 1a-k) were designed and synthesized, in which the 3-phosphocholine portion of platelet-activating factor (1-alkyl-2-acetyl-sn-glycero-3-phosphocholine, PAF) was replaced by the 2-(2-trimethylammonioethoxy)ethyl group and congeneric groups having oligo(ethyleneoxy)ethyl bridges of various lengths at position 3, together with modification at position 2 (lower alkyl, acetonyl, acetoacetyl, carboxymethyl and pyrimidin-2-yl groups). These ether lipids, characterized by a nonphosphorus lysoglycerolipid structure, showed potent antitumor activity in vitro (human promyelocytic leukemia cells, HL-60, and human epidermoid carcinoma cells, KB) and in vivo (mouse sarcoma S180 and mouse mammary carcinoma MM46). Maximal in vitro potency was obtained with 1-O-octadecyl-2-O-(2-pyrimidinyl)-3-O-[2-(2-trimethylammonioethoxy )ethyl] glycerol (1g; IC50 values for both HL-60 and KB were 0.32 microgram/ml, indicating a higher activity than alkyl-lysophospholipid, ET18-OMe). Several appropriately 2-substituted 1-octadecylglycerolipids with the 3-[2-(2-trimethylammonioethoxy)ethyl] group (e.g., methyl, 1b; butyl, 1f; 2,2,2-trifluoroethyl, 1j; and acetonyl, 1k) showed a potent life-span-prolonging effect on mice with ascites sarcoma S180 and on those with mammary carcinoma MM46, when administered intraperitoneally at 16.5 and 12.5 mg/kg/d, respectively. Compounds 1b and 1k showed definite tumor growth inhibition against solid sarcoma S180 in mice, whether given p.o. or i.v. at 16.5 mg/kg/d. Studies on the structure-activity relationships indicate that the metabolic stability to phospholipase C or related enzymes is at least partly responsible for the potent antitumor activity of this series of ether lipids.

  1. Subchronic Toxicity Study in Rats of Two New Ethyl-Carbamates with Ixodicidal Activity

    PubMed Central

    Prado-Ochoa, María Guadalupe; Abrego-Reyes, Víctor Hugo; Velázquez-Sánchez, Ana María; Muñoz-Guzmán, Marco Antonio; Ramírez-Noguera, Patricia; Angeles, Enrique; Alba-Hurtado, Fernando

    2014-01-01

    Female and male Wistar rats were used to determine the subchronic oral toxicities of two new ethyl-carbamates with ixodicidal activities (ethyl-4-bromphenyl-carbamate and ethyl-4-chlorphenyl-carbamate). The evaluated carbamates were administered in the drinking water (12.5, 25 and 50 mg/kg/day) for 90 days. Exposure to the evaluated carbamates did not cause mortality or clinical signs and did not affect food consumption or weight gain. However, exposure to these carbamates produced alterations in water consumption, hematocrit, percentages of reticulocytes, plasma proteins, some biochemical parameters (aspartate aminotransferase, gamma-glutamyl transpeptidase, cholinesterase, and creatinine activities), thiobarbituric acid reactive substances, and the relative weight of the spleen. Histologically, slight pathological alterations were found in the liver that were consistent with the observed biochemical alterations. The nonobserved adverse effect levels (NOAELs) of the evaluated carbamates were 12.5 mg/kg/day for both the female and male rats. The low severity and reversibility of the majority of the observed alterations suggest that the evaluated carbamates have low subchronic toxicity. PMID:24818142

  2. Mechanistic Insights on C-O and C-C Bond Activation and Hydrogen Insertion during Acetic Acid Hydrogenation Catalyzed by Ruthenium Clusters in Aqueous Medium

    SciTech Connect

    Shangguan, Junnan; Olarte, Mariefel V.; Chin, Ya-Huei

    2016-06-07

    Catalytic pathways for acetic acid (CH3COOH) and hydrogen (H2) reactions on dispersed Ru clusters in the aqueous medium and the associated kinetic requirements for C-O and C-C bond cleavages and hydrogen insertion are established from rate and isotopic assessments. CH3COOH reacts with H2 in steps that either retain its carbon backbone and lead to ethanol, ethyl acetate, and ethane (47-95 %, 1-23 %, and 2-17 % carbon selectivities, respectively) or break its C-C bond and form methane (1-43 % carbon selectivities) at moderate temperatures (413-523 K) and H2 pressures (10-60 bar, 298 K). Initial CH3COOH activation is the kinetically relevant step, during which CH3C(O)-OH bond cleaves on a metal site pair at Ru cluster surfaces nearly saturated with adsorbed hydroxyl (OH*) and acetate (CH3COO*) intermediates, forming an adsorbed acetyl (CH3CO*) and hydroxyl (OH*) species. Acetic acid turnover rates increase proportionally with both H2 (10-60 bar) and CH3COOH concentrations at low CH3COOH concentrations (<0.83 M), but decrease from first to zero order as the CH3COOH concentration and the CH3COO* coverages increase and the vacant Ru sites concomitantly decrease. Beyond the initial CH3C(O)-OH bond activation, sequential H-insertions on the surface acetyl species (CH3CO*) lead to C2 products and their derivative (ethanol, ethane, and ethyl acetate) and the competitive C-C bond cleavage of CH3CO* causes the eventual methane formation. The instantaneous carbon selectivities towards C2 species (ethanol, ethane, and ethyl acetate) increase linearly with the concentration of proton-type Hδ+ (derived from carboxylic acid dissociation) and chemisorbed H*. The selectivities towards C2 products decrease with increasing temperature, because of higher observed barriers for C-C bond cleavage than H-insertion. This study offers an interpretation of mechanism and energetics and provides kinetic evidence of carboxylic acid assisted proton-type hydrogen (Hδ+) shuffling during H

  3. Effect of acetic acid on lipid accumulation by glucose-fed activated sludge cultures

    SciTech Connect

    Mondala, Andro; Hernandez, Rafael; French, Todd; McFarland, Linda; Sparks, Darrell; Holmes, William; Haque, Monica

    2012-01-01

    The effect of acetic acid, a lignocellulose hydrolysis by-product, on lipid accumulation by activated sludge cultures grown on glucose was investigated. This was done to assess the possible application of lignocellulose as low-cost and renewable fermentation substrates for biofuel feedstock production. Results: Biomass yield was reduced by around 54% at a 2 g L -1 acetic acid dosage but was increased by around 18% at 10 g L -1 acetic acid dosage relative to the control run. The final gravimetric lipid contents at 2 and 10 g L -1 acetic acid levels were 12.5 + 0.7% and 8.8 + 3.2% w/w, respectively, which were lower than the control (17.8 + 2.8% w/w). However, biodiesel yields from activated sludge grown with acetic acid (5.6 + 0.6% w/w for 2 g L -1 acetic acid and 4.2 + 3.0% w/w for 10 g L -1 acetic acid) were higher than in raw activated sludge (1-2% w/w). The fatty acid profiles of the accumulated lipids were similar with conventional plant oil biodiesel feedstocks. Conclusions: Acetic acid enhanced biomass production by activated sludge at high levels but reduced lipid production. Further studies are needed to enhance acetic acid utilization by activated sludge microorganisms for lipid biosynthesis.

  4. Development of an antimicrobial material based on a nanocomposite cellulose acetate film for active food packaging.

    PubMed

    Rodríguez, Francisco J; Torres, Alejandra; Peñaloza, Ángela; Sepúlveda, Hugo; Galotto, María J; Guarda, Abel; Bruna, Julio

    2014-01-01

    Nanocomposites based on biopolymers have been recognised as potential materials for the development of new ecofriendly food packaging. In addition, if these materials incorporate active substances in their structure, the potential applications are much higher. Therefore, this work was oriented to develop nanocomposites with antimicrobial activity based on cellulose acetate (CA), a commercial organoclay Cloisite30B (C30B), thymol (T) as natural antimicrobial component and tri-ethyl citrate (TEC) as plasticiser. Nanocomposites were prepared by a solvent casting method and consisted of 5% (w/w) of C30B, 5% (w/w) of TEC and variable content of T (0%, 0.5% and 2% w/w). To evaluate the effect of C30B into the CA matrix, CA films without this organoclay but with T were also prepared. All nanocomposites showed the intercalation of CA into the organoclay structure; furthermore this intercalation was favoured when 2% (w/w) of T was added to the nanocomposite. In spite of the observed intercalation, the presence of C30B inside the CA matrices increased the opacity of the films significantly. On the other hand, T showed a plasticiser effect on the thermal properties of CA nanocomposites decreasing glass transition, melting temperature and melting enthalpy. The presence of T in CA nanocomposites also allowed the control de Listeria innocua growth when these materials were placed in contact with this Gram-positive bacterium. Interestingly, antimicrobial activity was increased with the presence of C30B. Finally, studies on T release showed that the clay structure inside the CA matrix did not affect its release rate; however, this nanofiller affected the partition coefficient KP/FS which was higher to CA nanocomposites films than in CA films without organoclay. The results obtained in the present study are really promising to be applied in the manufacture of food packaging materials.

  5. Diminution of Hepatic Response to 7, 12-dimethylbenz(α)anthracene by Ethyl Acetate Fraction of Acacia catechu Willd. through Modulation of Xenobiotic and Anti-Oxidative Enzymes in Rats

    PubMed Central

    Kumar, Rakesh; Kaur, Rajbir; Singh, Amrit Pal; Arora, Saroj

    2014-01-01

    Background Liver is the primary metabolizing site of body and is prone to damage by exogenous as well as endogenous intoxicants. Polycyclic aromatic hydrocarbons such as 7, 12- dimethylbenz(α)anthracene (DMBA) is an exogenous hepatotoxin, which is well known for modulating phase I, II and anti-oxidative enzymes of liver. Plants contain plethora of polyphenolic compounds which can reverse the damaging effect of various xenobiotics. The present study investigated protective role of the ethyl acetate fraction of Acacia catechu Willd. (EAF) against DMBA induced alteration in hepatic metabolizing and anti-oxidative enzymes in rats. Methodology and Principal Findings The rats were subjected to hepatic damage by treating with DMBA for 7 weeks on alternative days and treatment schedule was terminated at the end of 14 weeks. The rats were euthanized at the end of protocol and livers were homogenized. The liver homogenates were used to analyse phase I (NADPH-cytochrome P450 reducatse, NADH-cytochrome b5 reductase, cytochrome P420, cytochrome b5), phase II (glutathione-S-transferase, DT diaphorase and γ-Glutamyl transpeptidase) and antioxidative enzymes (catalase, superoxide dismutase, ascorbate peroxidase, glutathione reductase, guiacol peroxidase and lactate dehydrogenase). Furthermore, other oxidative stress parameters (thiobarbituric acid reactive substances, lipid hydroperoxides and conjugated dienes and reduced glutathione) and liver marker enzymes (serum glutamic oxaloacetic transaminase, serum glutamic pyruvic transaminase and alkaline phosphatase) were also studied. The DMBA induced significant changes in activity of hepatic enzymes that was reversed by treatment with three dose levels of EAF. Conclusion It is concluded that EAF affords hepato-protection against DMBA in rats through modulation of phase I, II and anti-oxidative enzymes. PMID:24587216

  6. Anti-wrinkle effects of Sargassum muticum ethyl acetate fraction on ultraviolet B-irradiated hairless mouse skin and mechanistic evaluation in the human HaCaT keratinocyte cell line.

    PubMed

    Song, Jae Hyoung; Piao, Mei Jing; Han, Xia; Kang, Kyoung Ah; Kang, Hee Kyoung; Yoon, Weon Jong; Ko, Mi Hee; Lee, Nam Ho; Lee, Mi Young; Chae, Sungwook; Hyun, Jin Won

    2016-10-01

    The present study investigated the photoprotective properties of the ethyl acetate fraction of Sargassum muticum (SME) against ultraviolet B (UVB)‑induced skin damage and photoaging in a mouse model. HR‑1 strain hairless male mice were divided into three groups: An untreated control group, a UVB‑irradiated vehicle group and a UVB‑irradiated SME group. The UVB‑irradiated mice in the SME group were orally administered with SME (100 mg/kg body weight in 0.1 ml water per day) and then exposed to radiation at a dose of 60‑120 mJ/cm2. Wrinkle formation and skin damage were evaluated by analysis of skin replicas, epidermal thickness and collagen fiber integrity in the dermal connective tissue. The mechanism underlying the action of SME was also investigated in the human HaCaT keratinocyte cell line following exposure of the cells to UVB at a dose of 30 mJ/cm2. The protein expression levels and activity of matrix metalloproteinase‑1 (MMP‑1), and the binding of activator protein‑1 (AP‑1) to the MMP‑1 promoter were assessed in the HaCaT cells using western blot analysis, an MMP‑1 fluorescent assay and a chromatin immune‑precipitation assay, respectively. The results showed that the mean length and depth of the wrinkles in the UVB‑exposed hairless mice were significantly improved by oral administration of SME, which also prevented the increase in epidermal thickness triggered by UVB irradiation. Furthermore, a marked increase in collagen bundle formation was observed in the UVB‑treated mice with SME administration. SME pretreatment also significantly inhibited the UVB‑induced upregulation in the expression and activity of MMP‑1 in the cultured HaCaT keratinocytes, and the UVB‑enhanced association of AP‑1 with the MMP‑1 promoter. These results suggested that SME may be useful as an anti-photoaging resource for the skin.

  7. Synthesis, Characterization, Antimicrobial and Antitumor Activities of Sucrose Octa(N-ethyl)carbamate.

    PubMed

    Raposo, Claudia D; Petrova, Krasimira T; Barros, Maria T; Calhelha, Ricardo C; Sokovic, Marina; Ferreira, Isabel C F R

    2016-01-01

    Sucrose octa(N-ethyl)carbamate was synthesized directly from sucrose and ethyl isocyanate, and its structure was confirmed by various analytical methods, such as (1)H and (13)C NMR, FTIR, m.p., MS, and optical rotation. Its antibacterial, antifungal and cytotoxic activities were investigated. It exhibited strong inhibition against all bacteria tested, namely S. aureus (MIC 0.18±0.006), B. cereus (MIC 0.094±0.000), M. flavus (MIC 0.28±0.01), L. monocytogenes (MIC 0.18±0.006), P. aeruginosa (MIC 0.094±0.002), S. typhimurium (MIC 0.094±0.002), E. coli (MIC 0.18±0.006) and E. cloacae (MIC 0.18±0.006) and strong antifungal activity towards T. viride (MIC 0.09 ± 0.006), A. versicolor (MIC 0.18 ± 0.01), A. ochraceus (MIC 0.375 ± 0.01) and P. ochrochloron (MIC 0.375 ± 0.04). Furthermore, it showed moderate antitumor potential against human breast (GI50 357.20±14.12), colon (GI50 332.43±11.19) and cervical (GI50 282.67±3.97) cell lines and, more important, without hepatotoxicity.

  8. Antimicrobial and antioxidant activities of clove essential oil and eugenyl acetate produced by enzymatic esterification.

    PubMed

    Vanin, Adriana B; Orlando, Tainara; Piazza, Suelen P; Puton, Bruna M S; Cansian, Rogério L; Oliveira, Debora; Paroul, Natalia

    2014-10-01

    This work reports the maximization of eugenyl acetate production by esterification of essential oil of clove in a solvent-free system using Novozym 435 as catalyst. The antimicrobial and antioxidant activities of clove essential oil and eugenyl acetate produced were determined. The conditions that maximized eugenyl acetate production were 60 °C, essential oil of clove to acetic anhydride ratio of 1:5, 150 rpm, and 10 wt% of enzyme, with a conversion of 99.87 %. A kinetic study was performed to assess the influence of substrates' molar ratio, enzyme concentration, and temperature on product yield. Results show that an excess of anhydride, enzyme concentration of 5.5 wt%, 50 °C, and essential oil of clove to acetic anhydride ratio of 1:5 afforded nearly a complete conversion after 2 h of reaction. Comparing the antibacterial activity of the essential oil of clove before and after esterification, we observed a decrease in the antimicrobial activity of eugenyl acetate, particularly with regard to minimum inhibitory concentration (MIC). Both eugenyl acetate and clove essential oil were most effective to the gram-negative than gram-positive bacteria group. The results showed a high antioxidant potential for essential oil before and particularly after the esterification reaction thus becoming an option for the formulation of new antioxidant products.

  9. Synthesis of high specific activity [ethyl-1,2-3H]-labeled chlorpyrifos oxon and diazoxon

    SciTech Connect

    Zhang, Nanjing; Morimoto, Hiromi; Williams, Philip G.; Casida, John E

    2000-05-01

    [Ethyl-1,2-3H] Chlorpyrifos oxon and [ethyl-1,2-3H] diazoxon were synthesized at a specific activity of 79 and 58 Ci/mmol, respectively, by catalytic tritiation of the corresponding monovinyl analogs over Pd/C. Direct evidence is provided that the high specific activity results from isotope exchange of the terminal vinylic protons prior to saturation of the double bond. This radiosynthesis procedure is applicable to the toxicologically-important oxon metabolites of many commercial O-O-diethyl phosphorothioate pesticides.

  10. Genotoxicity and cytotoxicity assessment of new ethyl-carbamates with ixodicidal activity.

    PubMed

    Prado-Ochoa, María Guadalupe; Muñoz-Guzmán, Marco Antonio; Vázquez-Valadez, Víctor Hugo; Velázquez-Sánchez, Ana María; Salazar, Ana María; Ramírez-Noguera, Patricia; Angeles, Enrique; Alba-Hurtado, Fernando

    2016-09-01

    The mammalian erythrocyte micronucleus test was used on the peripheral blood of Wistar rats exposed to two new ethyl-carbamates: ethyl-4-bromophenyl-carbamate (LQM 919) and ethyl-4-chlorophenyl-carbamate (LQM 996) to analyze their genotoxic potential. The mitotic index and cell proliferation kinetics in human lymphocyte cultures in the presence of these ethyl-carbamates were used to evaluate cytotoxicity and cytostaticity respectively. Exposure to greater acute doses (300mg/kg) and to all of the subchronic doses (12.5, 25 and 50mg/kg daily for 90 days) of these ethyl-carbamates induced an increased frequency (p<0.05) of micro-nucleated polychromatic erythrocytes (MN-PCE) compared with rats not exposed to the ethyl-carbamates. Increases in MN-PCE was higher in males than in females exposed to LQM 996 50mg/Kg (p<0.05). All observed changes in rats return 21days after suspending ethyl-carbamate exposure. The highest concentration (0.3mM) of both ethyl-carbamates in lymphocyte cultures increased the percentage of cells in first division metaphase and decreased the percentage of cells in third division metaphase, indicating an increase in cell cycle length or a possible cell cycle arrest in metaphase (cytostatic effect). The results of this study show that the evaluated ethyl-carbamates may induce genotoxic damage in rats and alterations in the human lymphocyte cell cycle.

  11. Effects of glucose on the performance of enhanced biological phosphorus removal activated sludge enriched with acetate.

    PubMed

    Gebremariam, Seyoum Yami; Beutel, Marc W; Christian, David; Hess, Thomas F

    2012-10-01

    The effects of glucose on enhanced biological phosphorus removal (EBPR) activated sludge enriched with acetate was investigated using sequencing batch reactors. A glucose/acetate mixture was serially added to the test reactor in ratios of 25/75%, 50/50%, and 75/25% and the EBPR activity was compared to the control reactor fed with 100% acetate. P removal increased at a statistically significant level to a near-complete in the test reactor when the mixture increased to 50/50%. However, EBPR deteriorated when the glucose/acetate mixture increased to 75/25% in the test reactor and when the control reactor abruptly switched to 100% glucose. These results, in contrast to the EBPR conventional wisdom, suggest that the addition of glucose at moderate levels in wastewaters does not impede and may enhance EBPR, and that glucose waste products should be explored as an economical sustainable alternative when COD enhancement of EBPR is needed.

  12. Activation of AMP-Activated Protein Kinase and Stimulation of Energy Metabolism by Acetic Acid in L6 Myotube Cells.

    PubMed

    Maruta, Hitomi; Yoshimura, Yukihiro; Araki, Aya; Kimoto, Masumi; Takahashi, Yoshitaka; Yamashita, Hiromi

    2016-01-01

    Previously, we found that orally administered acetic acid decreased lipogenesis in the liver and suppressed lipid accumulation in adipose tissue of Otsuka Long-Evans Tokushima Fatty rats, which exhibit hyperglycemic obesity with hyperinsulinemia and insulin resistance. Administered acetic acid led to increased phosphorylation of AMP-activated protein kinase (AMPK) in both liver and skeletal muscle cells, and increased transcripts of myoglobin and glucose transporter 4 (GLUT4) genes in skeletal muscle of the rats. It was suggested that acetic acid improved the lipid metabolism in skeletal muscles. In this study, we examined the activation of AMPK and the stimulation of GLUT4 and myoglobin expression by acetic acid in skeletal muscle cells to clarify the physiological function of acetic acid in skeletal muscle cells. Acetic acid added to culture medium was taken up rapidly by L6 cells, and AMPK was phosphorylated upon treatment with acetic acid. We observed increased gene and protein expression of GLUT4 and myoglobin. Uptake of glucose and fatty acids by L6 cells were increased, while triglyceride accumulation was lower in treated cells compared to untreated cells. Furthermore, treated cells also showed increased gene and protein expression of myocyte enhancer factor 2A (MEF2A), which is a well-known transcription factor involved in the expression of myoglobin and GLUT4 genes. These results indicate that acetic acid enhances glucose uptake and fatty acid metabolism through the activation of AMPK, and increases expression of GLUT4 and myoglobin.

  13. Activation of AMP-Activated Protein Kinase and Stimulation of Energy Metabolism by Acetic Acid in L6 Myotube Cells

    PubMed Central

    Maruta, Hitomi; Yoshimura, Yukihiro; Araki, Aya; Kimoto, Masumi; Takahashi, Yoshitaka; Yamashita, Hiromi

    2016-01-01

    Previously, we found that orally administered acetic acid decreased lipogenesis in the liver and suppressed lipid accumulation in adipose tissue of Otsuka Long-Evans Tokushima Fatty rats, which exhibit hyperglycemic obesity with hyperinsulinemia and insulin resistance. Administered acetic acid led to increased phosphorylation of AMP-activated protein kinase (AMPK) in both liver and skeletal muscle cells, and increased transcripts of myoglobin and glucose transporter 4 (GLUT4) genes in skeletal muscle of the rats. It was suggested that acetic acid improved the lipid metabolism in skeletal muscles. In this study, we examined the activation of AMPK and the stimulation of GLUT4 and myoglobin expression by acetic acid in skeletal muscle cells to clarify the physiological function of acetic acid in skeletal muscle cells. Acetic acid added to culture medium was taken up rapidly by L6 cells, and AMPK was phosphorylated upon treatment with acetic acid. We observed increased gene and protein expression of GLUT4 and myoglobin. Uptake of glucose and fatty acids by L6 cells were increased, while triglyceride accumulation was lower in treated cells compared to untreated cells. Furthermore, treated cells also showed increased gene and protein expression of myocyte enhancer factor 2A (MEF2A), which is a well-known transcription factor involved in the expression of myoglobin and GLUT4 genes. These results indicate that acetic acid enhances glucose uptake and fatty acid metabolism through the activation of AMPK, and increases expression of GLUT4 and myoglobin. PMID:27348124

  14. Parameters Affecting Ethyl Ester Production by Saccharomyces cerevisiae during Fermentation▿

    PubMed Central

    Saerens, S. M. G.; Delvaux, F.; Verstrepen, K. J.; Van Dijck, P.; Thevelein, J. M.; Delvaux, F. R.

    2008-01-01

    Volatile esters are responsible for the fruity character of fermented beverages and thus constitute a vital group of aromatic compounds in beer and wine. Many fermentation parameters are known to affect volatile ester production. In order to obtain insight into the production of ethyl esters during fermentation, we investigated the influence of several fermentation variables. A higher level of unsaturated fatty acids in the fermentation medium resulted in a general decrease in ethyl ester production. On the other hand, a higher fermentation temperature resulted in greater ethyl octanoate and decanoate production, while a higher carbon or nitrogen content of the fermentation medium resulted in only moderate changes in ethyl ester production. Analysis of the expression of the ethyl ester biosynthesis genes EEB1 and EHT1 after addition of medium-chain fatty acid precursors suggested that the expression level is not the limiting factor for ethyl ester production, as opposed to acetate ester production. Together with the previous demonstration that provision of medium-chain fatty acids, which are the substrates for ethyl ester formation, to the fermentation medium causes a strong increase in the formation of the corresponding ethyl esters, this result further supports the hypothesis that precursor availability has an important role in ethyl ester production. We concluded that, at least in our fermentation conditions and with our yeast strain, the fatty acid precursor level rather than the activity of the biosynthetic enzymes is the major limiting factor for ethyl ester production. The expression level and activity of the fatty acid biosynthetic enzymes therefore appear to be prime targets for flavor modification by alteration of process parameters or through strain selection. PMID:17993562

  15. Kinetics of the reactions of chlorine atoms with a series of acetates

    NASA Astrophysics Data System (ADS)

    Xing, Jia-Hua; Takahashi, Kenshi; Hurley, Michael D.; Wallington, Timothy J.

    2009-06-01

    The kinetics of the reactions of Cl atoms with a series of alkyl acetates were investigated using relative and absolute rate methods in 2-700 Torr of N 2 at room temperature. Consistent results were obtained using the two methods. The data from the absolute rate measurements were more precise and were (in units of 10 -11 cm 3 molecule -1 s -1): ethyl acetate, 1.76 ± 0.11; n-propyl acetate, 7.19 ± 0.11; i-propyl acetate, 1.97 ± 0.24; n-butyl acetate, 15.8 ± 0.94; i-butyl acetate, 9.97 ± 0.60; s-butyl acetate, 8.01 ± 0.48; and t-butyl acetate, 1.64 ± 0.10. The reactivity of alkyl acetates is discussed in terms of structure-activity relationship.

  16. Anti-inflammatory activity of methyl palmitate and ethyl palmitate in different experimental rat models

    SciTech Connect

    Saeed, Noha M.; El-Demerdash, Ebtehal; Abdel-Rahman, Hanaa M.; Algandaby, Mardi M.; Al-Abbasi, Fahad A.; Abdel-Naim, Ashraf B.

    2012-10-01

    Methyl palmitate (MP) and ethyl palmitate (EP) are naturally occurring fatty acid esters reported as inflammatory cell inhibitors. In the current study, the potential anti-inflammatory activity of MP and EP was evaluated in different experimental rat models. Results showed that MP and EP caused reduction of carrageenan-induced rat paw edema in addition to diminishing prostaglandin E2 (PGE2) level in the inflammatory exudates. In lipopolysaccharide (LPS)-induced endotoxemia in rats, MP and EP reduced plasma levels of tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6). MP and EP decreased NF-κB expression in liver and lung tissues and ameliorated histopathological changes caused by LPS. Topical application of MP and EP reduced ear edema induced by croton oil in rats. In the same animal model, MP and EP reduced neutrophil infiltration, as indicated by decreased myeloperoxidase (MPO) activity. In conclusion, this study demonstrates the effectiveness of MP and EP in combating inflammation in several experimental models. -- Highlights: ► Efficacy of MP and EP in combating inflammation was displayed in several models. ► MP and EP reduced carrageenan-induced rat paw edema and prostaglandin E2 level. ► MP and EP decreased TNF-α and IL-6 levels in experimental endotoxemia. ► MP and EP reduced NF-κB expression and histological changes in rat liver and lung. ► MP and EP reduced croton oil-induced ear edema and neutrophil infiltration.

  17. Anti-inflammatory activity of methyl palmitate and ethyl palmitate in different experimental rat models.

    PubMed

    Saeed, Noha M; El-Demerdash, Ebtehal; Abdel-Rahman, Hanaa M; Algandaby, Mardi M; Al-Abbasi, Fahad A; Abdel-Naim, Ashraf B

    2012-10-01

    Methyl palmitate (MP) and ethyl palmitate (EP) are naturally occurring fatty acid esters reported as inflammatory cell inhibitors. In the current study, the potential anti-inflammatory activity of MP and EP was evaluated in different experimental rat models. Results showed that MP and EP caused reduction of carrageenan-induced rat paw edema in addition to diminishing prostaglandin E2 (PGE2) level in the inflammatory exudates. In lipopolysaccharide (LPS)-induced endotoxemia in rats, MP and EP reduced plasma levels of tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6). MP and EP decreased NF-κB expression in liver and lung tissues and ameliorated histopathological changes caused by LPS. Topical application of MP and EP reduced ear edema induced by croton oil in rats. In the same animal model, MP and EP reduced neutrophil infiltration, as indicated by decreased myeloperoxidase (MPO) activity. In conclusion, this study demonstrates the effectiveness of MP and EP in combating inflammation in several experimental models.

  18. Effects of chlorpyrifos ethyl on acetylcholinesterase activity in climbing perch cultured in rice fields in the Mekong Delta, Vietnam.

    PubMed

    Nguyen, Tam Thanh; Berg, Håkan; Nguyen, Hang Thi Thuy; Nguyen, Cong Van

    2015-07-01

    Climbing perch is commonly harvested in rice fields and associated wetlands in the Mekong Delta. Despite its importance in providing food and income to local households, there is little information how this fish species is affected by the high use of pesticides in rice farming. Organophosphate insecticides, such as chlorpyrifos ethyl, which are highly toxic to aquatic organisms, are commonly used in the Mekong Delta. This study shows that the brain acetylcholinesterase (AChE) activity in climbing perch fingerlings cultured in rice fields, was significantly inhibited by a single application of chlorpyrifos ethyl, at doses commonly applied by rice farmers (0.32-0.64 kg/ha). The water concentration of chlorpyrifos ethyl decreased below the detection level within 3 days, but the inhibition of brain AChE activity remained for more than 12 days. In addition, the chlorpyrifos ethyl treatments had a significant impact on the survival and growth rates of climbing perch fingerlings, which were proportional to the exposure levels. The results indicate that the high use of pesticides among rice farmers in the Mekong Delta could have a negative impact on aquatic organisms and fish yields, with implications for the aquatic biodiversity, local people's livelihoods and the aquaculture industry in the Mekong Delta.

  19. Disproportionation and nuclease activity of bis[2-ethyl-2-hydroxybutanoato(2-)]oxochromate(V) in neutral aqueous solutions.

    PubMed

    Levina, A; Lay, P A; Dixon, N E

    2000-02-07

    Complex 1, [Cr(V)O(ehba)2]- (ehba = 2-ethyl-2-hydroxybutanoate(2-)) is the most studied model compound of relevance to the biological activity of Cr(V) with regard to Cr-induced cancers. The first detailed kinetic study of disproportionation of 1 under neutral pH conditions (pH 6.0-8.0, [NaClO4] = 1.0 M, 37 degrees C) is reported. Kinetic data were collected by stopped-flow and conventional UV-vis spectroscopies and processed by the global analysis method. The disproportionation, which follows the stoichiometry 3Cr(V) --> 2Cr(VI) + Cr(III) (1), leads to release of 5 mol of H+/3 mol of Cr(V). Reaction 1 is accelerated by phosphate, but is not affected by acetate, HEPES, or Tris buffers. Initial rates of Cr(V) decay are directly proportional to [Cr(V)]0 (0.020-1.0 mM); they increase with an increase in the pH values and decrease in the presence of a large excess of ehba ligand. The first direct evidence for the formation of Cr(IV) intermediates in reaction 1 has been obtained; however, their UV-vis spectral properties were different from those of the well-characterized Cr(IV)-ehba complexes. The Cr(III) products of reaction I in phosphate buffers differ from those in the other buffers. A mechanism is proposed for reaction 1 on the basis of kinetic modeling. Influences of the reaction time and conditions on the extent of plasmid DNA cleavage induced by 1 have been studied under conditions corresponding to those of the kinetic studies. A comparison of the kinetic and DNA cleavage results has shown that direct interaction of 1 with the phosphate backbone of DNA is the most likely first step in the mechanism of DNA cleavage in neutral media. Small additions of Mn(II) ((0.01-0.1)[Cr(V)]0) did not affect the rate and stoichiometry of reaction 1, but suppressed the formation of Cr(IV) intermediates (presumably due to the catalysis of Cr(IV) disproportionation). However, much higher concentrations of Mn(II) ((0.1-1.0)[Cr(V)]0) were required to inhibit DNA cleavage induced by

  20. The Antibacterial Activity of Acetic Acid against Biofilm-Producing Pathogens of Relevance to Burns Patients

    PubMed Central

    Halstead, Fenella D.; Rauf, Maryam; Moiemen, Naiem S.; Bamford, Amy; Wearn, Christopher M.; Fraise, Adam P.; Lund, Peter A.; Oppenheim, Beryl A.; Webber, Mark A.

    2015-01-01

    Introduction Localised infections, and burn wound sepsis are key concerns in the treatment of burns patients, and prevention of colonisation largely relies on biocides. Acetic acid has been shown to have good antibacterial activity against various planktonic organisms, however data is limited on efficacy, and few studies have been performed on biofilms. Objectives We sought to investigate the antibacterial activity of acetic acid against important burn wound colonising organisms growing planktonically and as biofilms. Methods Laboratory experiments were performed to test the ability of acetic acid to inhibit growth of pathogens, inhibit the formation of biofilms, and eradicate pre-formed biofilms. Results Twenty-nine isolates of common wound-infecting pathogens were tested. Acetic acid was antibacterial against planktonic growth, with an minimum inhibitory concentration of 0.16–0.31% for all isolates, and was also able to prevent formation of biofilms (at 0.31%). Eradication of mature biofilms was observed for all isolates after three hours of exposure. Conclusions This study provides evidence that acetic acid can inhibit growth of key burn wound pathogens when used at very dilute concentrations. Owing to current concerns of the reducing efficacy of systemic antibiotics, this novel biocide application offers great promise as a cheap and effective measure to treat infections in burns patients. PMID:26352256

  1. Salt-enhanced removal of 2-ethyl-1-hexanol from aqueous solutions by adsorption on activated carbon.

    PubMed

    Chang, Ganggang; Bao, Zongbi; Zhang, Zhiguo; Xing, Huabin; Su, Baogen; Yang, Yiwen; Ren, Qilong

    2013-12-15

    2-Ethyl-1-hexanol has extensive industrial applications in solvent extraction, however, in view of its potential pollution to environment, the removal and recovery of 2-ethyl-1-hexanol is considered an essential step toward its sustainable use in the future. In this work, we report the removal of 2-ethyl-1-hexanol from aqueous solutions containing salts in high concentrations by adsorption on a coal-based activated carbon. Adsorption thermodynamics showed that the experimental isotherms were conformed well to the Langmuir equation. Also it was found that inorganic salts, i.e. MgCl2 and CaCl2 in high concentration significantly enhanced the adsorption capacity from 223 mg/g in the deionized water to 277 mg/g in a saline water. This phenomenon of adsorption enhancement could be ascribed to the salt-out effect. Kinetic analysis indicated that adsorption kinetics follows the pseudo-second-order equation and the adsorption rate constants increase with the salt concentration. The dynamic breakthrough volume and adsorbed amount of 2-ethyl-1-hexanol were significantly elevated when the salt is present in the water. The dynamic saturated adsorption amount increased from 218.3mg/g in the deionized water to 309.5mg/g in a salt lake brine. The Tomas model was well applied to predict the breakthrough curves and determine the characteristics parameters of the adsorption column.

  2. Validation and uncertainty analysis of a multiresidue method for 42 pesticides in made tea, tea infusion and spent leaves using ethyl acetate extraction and liquid chromatography-tandem mass spectrometry.

    PubMed

    Kanrar, Bappaditya; Mandal, Sudeb; Bhattacharyya, Anjan

    2010-03-19

    A rapid, specific and sensitive multiresidue method to determine 42 pesticides in made tea, tea infusion and spent leaves has been developed and validated for the routine analysis by liquid chromatography-tandem mass spectrometry (LC-MS/MS). The method was reproducible (Horwitz ratio (HorRat) <0.5 at 50 ng/g) and validated by the analysis of sample spiked at 50 and 100 ng/g in made tea, tea infusion and spent leaves. The samples were extracted with ethyl acetate+cyclohexane (9:1; v/v), and the extracts were cleaned up by dispersive solid phase extraction with primary secondary amine sorbent+graphitized carbon black+Florisil. The recoveries of all the pesticides were between 70% and 120% with a relative standard deviation of less than 15% and correlation coefficient for each pesticide was R(2) > or =0.99. The matrix effect on signal of respective compounds was measured by comparing matrix-matched calibration standards with those in solvent-only. The limits of quantitation (LOQ) met the requirements of the maximum residue limits (MRLs) for pesticides in tea as recommended by the European Union.

  3. Development of Biocomposites with Antioxidant Activity Based on Red Onion Extract and Acetate Cellulose

    PubMed Central

    López de Dicastillo, Carol; Navarro, Rosa; Guarda, Abel; Galotto, Maria José

    2015-01-01

    Antioxidant biocomposites have been successfully developed from cellulose acetate, eco-friendly triethyl citrate plasticizer and onion extract as a source of natural antioxidants. First, an onion extraction process was optimized to obtain the extract with highest antioxidant power. Extracts under absolute ethanol and ethanol 85% were the extracts with the highest antioxidant activity, which were the characterized through different methods, DPPH (2,2-diphenyl-1-picrylhydrazyl) and ABTS (2,2ʹ-azinobis(3-ethylbenzothiazoline-6-sulphonate)), that measure radical scavenger activity, and polyphenolic and flavonoid content. Afterwards, the extract was incorporated in cellulose acetate as polymer matrix owing to develop an active material intended to oxidative sensitive food products packaging. Different concentrations of onion extract and plasticizer were statistically studied by using response surface methodology in order to analyze the influence of both factors on the release of active compounds and therefore the antioxidant activity of these materials. PMID:26783842

  4. Laser vibrational overtone activation of ethyl acrylate/benzoyl peroxide mixture

    NASA Astrophysics Data System (ADS)

    Grinevich, Oleg; Snavely, D. L.

    1999-04-01

    Intra- and extracavity laser vibrational overtone polymerization of ethyl acrylate/benzoyl peroxide mixture has been demonstrated. Five photolysis wavenumbers on and near the fifth CH stretch overtone absorption of benzoyl peroxide was investigated. The polymer yield was monitored by observing the decrease in the intensity ratio of the olefinic/methyl and methylenic first CH stretch overtone absorptions of ethyl acrylate. The rate of the polymerization did not depend on the photolysis wavenumber. Molecular weights of the overtone initiated polymers were an order of magnitude larger than those obtained by thermal polymerization. The polymerization rate is compared to the intracavity laser vibrational overtone polymerization of methyl methacrylate.

  5. Crystal structure of (Z)-ethyl 2-{5-[(2-benzyl­idene-3-oxo-2,3-di­hydro­benzo[b][1,4]thia­zin-4-yl)meth­yl]-1H-1,2,3-triazol-1-yl}acetate

    PubMed Central

    Ellouz, M.; Sebbar, N. K.; Essassi, E. M.; Ouzidan, Y.; Mague, J. T.

    2015-01-01

    The title compound, C22H20N4O3S, features two fused six-membered rings linked to a 1,2,3-triazole ring which is attached to an ethyl acetate group. The heterocycle in the benzo­thia­zine residue has an envelope conformation with the S atom being the flap. The conformation of the ethyl acetate side chain, which is directed to the same side of the mol­ecule as the C6 ring of the fused-ring system, may be partially established by a pair of weak intra­molecular C—H⋯O(carbon­yl) inter­actions. The three-dimensional packing is aided by inter­molecular C—H⋯O and C—H⋯N inter­actions. PMID:26870477

  6. Anti-angiogenic activity of a novel synthetic agent, 9alpha-fluoromedroxyprogesterone acetate.

    PubMed

    Yamaji, T; Tsuboi, H; Murata, N; Uchida, M; Kohno, T; Sugino, E; Hibino, S; Shimamura, M; Oikawa, T

    1999-10-18

    9Alpha-fluoromedroxyprogesterone acetate (FMPA) is a novel synthetic analog of medroxyprogesterone acetate (MPA), widely used as therapeutic agent for breast and endometrium cancers. FMPA showed almost the same binding affinities to the progesterone and glucocorticoid receptors as MPA. In the rabbit corneal assay, FMPA, MPA and fumagillin significantly inhibited the angiogenic response induced by rat mammary tumor at doses of 0. 1, 1 and 50 microg/pellet, respectively, so FMPA showed greater anti-angiogenic activity than MPA and fumagillin. In the mouse dorsal air sac method, FMPA inhibited the mouse sarcoma 180 cell-induced angiogenesis by oral administration at a dose of 200 mg/kg. FMPA inhibited the activity of plasminogen activator (PA) in bovine endothelial cells. These results suggest that FMPA may be useful for diseases associated with angiogenesis by oral administration.

  7. Isolation, transformation, anticancer, and apoptosis activity of lupeyl acetate from Artocarpus integra

    NASA Astrophysics Data System (ADS)

    Suwito, Hery; Heffen, Wan Lelly; Cahyana, Herry; Suwarso, Wahyudi Priyono

    2016-03-01

    Lupeyl acetate -a major constituent of the bark of Artocarpus integra- was isolated and then transformed chemically into lupeol and lupenone by hydrolysis and oxidation reaction respectively. The molecular structures of the prepared compounds were determined based on FTIR, MS and NMR spectrum evidences. Their anticancer activities were determined against breast cancer cells MCF-7 using neutral red assay, while their apoptotic activity were confirmed by flowcytometric analysis using Annexin V-FTIC assay and DNA fragmentation. The IC50 of Lupeyl acetate, lupeol, and lupenone were 48.79; 43.09; and 8.07 µg/mL respectively. The results of flowcytometric analysis and DNA fragmentation showed that anticancer activity of the prepared compounds following apoptosis mechanism.

  8. Acetic Acid, the Active Component of Vinegar, Is an Effective Tuberculocidal Disinfectant

    PubMed Central

    Cortesia, Claudia; Vilchèze, Catherine; Bernut, Audrey; Contreras, Whendy; Gómez, Keyla; de Waard, Jacobus; Jacobs, William R.; Kremer, Laurent; Takiff, Howard

    2014-01-01

    ABSTRACT Effective and economical mycobactericidal disinfectants are needed to kill both Mycobacterium tuberculosis and non-M. tuberculosis mycobacteria. We found that acetic acid (vinegar) efficiently kills M. tuberculosis after 30 min of exposure to a 6% acetic acid solution. The activity is not due to pH alone, and propionic acid also appears to be bactericidal. M. bolletii and M. massiliense nontuberculous mycobacteria were more resistant, although a 30-min exposure to 10% acetic acid resulted in at least a 6-log10 reduction of viable bacteria. Acetic acid (vinegar) is an effective mycobactericidal disinfectant that should also be active against most other bacteria. These findings are consistent with and extend the results of studies performed in the early and mid-20th century on the disinfectant capacity of organic acids. IMPORTANCE  Mycobacteria are best known for causing tuberculosis and leprosy, but infections with nontuberculous mycobacteria are an increasing problem after surgical or cosmetic procedures or in the lungs of cystic fibrosis and immunosuppressed patients. Killing mycobacteria is important because Mycobacterium tuberculosis strains can be multidrug resistant and therefore potentially fatal biohazards, and environmental mycobacteria must be thoroughly eliminated from surgical implements and respiratory equipment. Currently used mycobactericidal disinfectants can be toxic, unstable, and expensive. We fortuitously found that acetic acid kills mycobacteria and then showed that it is an effective mycobactericidal agent, even against the very resistant, clinically important Mycobacterium abscessus complex. Vinegar has been used for thousands of years as a common disinfectant, and if it can kill mycobacteria, the most disinfectant-resistant bacteria, it may prove to be a broadly effective, economical biocide with potential usefulness in health care settings and laboratories, especially in resource-poor countries. PMID:24570366

  9. Acetic Acid, the active component of vinegar, is an effective tuberculocidal disinfectant.

    PubMed

    Cortesia, Claudia; Vilchèze, Catherine; Bernut, Audrey; Contreras, Whendy; Gómez, Keyla; de Waard, Jacobus; Jacobs, William R; Kremer, Laurent; Takiff, Howard

    2014-02-25

    Effective and economical mycobactericidal disinfectants are needed to kill both Mycobacterium tuberculosis and non-M. tuberculosis mycobacteria. We found that acetic acid (vinegar) efficiently kills M. tuberculosis after 30 min of exposure to a 6% acetic acid solution. The activity is not due to pH alone, and propionic acid also appears to be bactericidal. M. bolletii and M. massiliense nontuberculous mycobacteria were more resistant, although a 30-min exposure to 10% acetic acid resulted in at least a 6-log10 reduction of viable bacteria. Acetic acid (vinegar) is an effective mycobactericidal disinfectant that should also be active against most other bacteria. These findings are consistent with and extend the results of studies performed in the early and mid-20th century on the disinfectant capacity of organic acids. IMPORTANCE Mycobacteria are best known for causing tuberculosis and leprosy, but infections with nontuberculous mycobacteria are an increasing problem after surgical or cosmetic procedures or in the lungs of cystic fibrosis and immunosuppressed patients. Killing mycobacteria is important because Mycobacterium tuberculosis strains can be multidrug resistant and therefore potentially fatal biohazards, and environmental mycobacteria must be thoroughly eliminated from surgical implements and respiratory equipment. Currently used mycobactericidal disinfectants can be toxic, unstable, and expensive. We fortuitously found that acetic acid kills mycobacteria and then showed that it is an effective mycobactericidal agent, even against the very resistant, clinically important Mycobacterium abscessus complex. Vinegar has been used for thousands of years as a common disinfectant, and if it can kill mycobacteria, the most disinfectant-resistant bacteria, it may prove to be a broadly effective, economical biocide with potential usefulness in health care settings and laboratories, especially in resource-poor countries.

  10. Assessment of Acute Oral and Dermal Toxicity of 2 Ethyl-Carbamates with Activity against Rhipicephalus microplus in Rats

    PubMed Central

    Prado-Ochoa, María Guadalupe; Gutiérrez-Amezquita, Ricardo Alfonso; Abrego-Reyes, Víctor Hugo; Velázquez-Sánchez, Ana María; Muñoz-Guzmán, Marco Antonio; Ramírez-Noguera, Patricia; Angeles, Enrique; Alba-Hurtado, Fernando

    2014-01-01

    The acute oral and dermal toxicity of two new ethyl-carbamates (ethyl-4-bromophenyl-carbamate and ethyl-4-chlorophenyl-carbamate) with ixodicide activity was determined in rats. The oral LD50 of each carbamate was 300 to 2000 mg/kg, and the dermal LD50 of each carbamate was >5000 mg/kg. Clinically, the surviving rats that had received oral doses of each carbamate showed decreased weight gain (P < 0.05) and had slight nervous system manifestations. These clinical signs were evident from the 300 mg/kg dose and were reversible, whereas the 2000 mg/kg dose caused severe damage and either caused their death or was motive for euthanasia. At necropsy, these rats had dilated stomachs and cecums with diffuse congestion, as well as moderate congestion of the liver. Histologically, the liver showed slight degenerative lesions, binucleated hepatocytes, focal coagulative necrosis, and congestion areas; the severity of the lesions increased with dosage. Furthermore, an slight increase in gamma-glutamyltransferase, lactate dehydrogenase, and creatinine was observed in the plasma. The dermal application of the maximum dose (5000 mg/kg) of each carbamate did not cause clinical manifestations or liver and skin alterations. This finding demonstrates that the carbamates under study have a low oral hazard and low acute dermal toxicity. PMID:24883331

  11. Assessment of acute oral and dermal toxicity of 2 ethyl-carbamates with activity against Rhipicephalus microplus in rats.

    PubMed

    Prado-Ochoa, María Guadalupe; Gutiérrez-Amezquita, Ricardo Alfonso; Abrego-Reyes, Víctor Hugo; Velázquez-Sánchez, Ana María; Muñoz-Guzmán, Marco Antonio; Ramírez-Noguera, Patricia; Angeles, Enrique; Alba-Hurtado, Fernando

    2014-01-01

    The acute oral and dermal toxicity of two new ethyl-carbamates (ethyl-4-bromophenyl-carbamate and ethyl-4-chlorophenyl-carbamate) with ixodicide activity was determined in rats. The oral LD50 of each carbamate was 300 to 2000 mg/kg, and the dermal LD50 of each carbamate was >5000 mg/kg. Clinically, the surviving rats that had received oral doses of each carbamate showed decreased weight gain (P < 0.05) and had slight nervous system manifestations. These clinical signs were evident from the 300 mg/kg dose and were reversible, whereas the 2000 mg/kg dose caused severe damage and either caused their death or was motive for euthanasia. At necropsy, these rats had dilated stomachs and cecums with diffuse congestion, as well as moderate congestion of the liver. Histologically, the liver showed slight degenerative lesions, binucleated hepatocytes, focal coagulative necrosis, and congestion areas; the severity of the lesions increased with dosage. Furthermore, an slight increase in gamma-glutamyltransferase, lactate dehydrogenase, and creatinine was observed in the plasma. The dermal application of the maximum dose (5000 mg/kg) of each carbamate did not cause clinical manifestations or liver and skin alterations. This finding demonstrates that the carbamates under study have a low oral hazard and low acute dermal toxicity.

  12. Degradation of ethyl paraben by heat-activated persulfate oxidation: statistical evaluation of operating factors and transformation pathways.

    PubMed

    Frontistis, Zacharias; Antonopoulou, Maria; Konstantinou, Ioannis; Mantzavinos, Dionissios

    2017-01-01

    A factorial design methodology was implemented to evaluate the importance of ethyl paraben (EP) concentration (500-1500 μg/L), sodium persulfate concentration (400-500 mg/L), temperature (40-60 °C), reaction time (2-30 min), water matrix (pure water or secondary treated wastewater), and initial solution pH (3-9) on EP removal by heat-activated persulfate oxidation. All individual effects, except the solution pH, were statistically significant and so were the second-order interactions of ethyl paraben concentration with temperature or the reaction time. The influence of the water matrix was crucial, and the efficiency of the process was lower in secondary treated wastewater due to the presence of natural organic matter and inorganic salts that compete with ethyl paraben for the reactive oxygen species. Liquid chromatography time-of-flight mass spectrometry (LC-TOF-MS) was employed to identify major transformation by-products (TBPs); 13 compounds were detected as TBPs of EP. Degradation occurred through (i) hydroxylation, (ii) dealkylation, and (iii) oligomerization reactions leading to TBPs with ether and biphenyl structures. Oligomerization reactions were found to be the dominant pathway during the first steps of the reaction. The toxicity of 500 μg/L EP in secondary treated wastewater was tested against marine bacteria Vibrio fischeri; toxicity increased during the first minutes due to the production of several TBPs, but it consistently decreased thereafter.

  13. Stereospecific ligands and their complexes. XX. Synthesis, characterization and antimicrobial activity of palladium(II) complexes with some alkyl esters of ethylenediamine-N,N‧-di-S,S-(2,2‧-dibenzyl)acetic acid

    NASA Astrophysics Data System (ADS)

    Dimitrijević, Dejana P.; Radić, Gordana P.; Jevtić, Verica V.; Mišić, Milena; Baskić, Dejan; Trifunović, Srećko R.

    2014-08-01

    Four new palladium(II) complexes of general formula [PdCl2(R2-S,S-eddba)] (R = ethyl, n-propyl, n-butyl and n-pentyl; S,S-eddba = ethylenediamine-N,N‧-di-S,S-(2,2‧-dibenzyl)acetate) have been synthesized and characterized by microanalysis, infrared, 1H and 13C NMR spectroscopy. In vitro antimicrobial activity for ligands L1-L4 general formula R2-S,S-eddba and complexes C1-C4 was investigated.

  14. Involvement of cytochrome P-450 enzyme activity in the selectivity and safening action of pyrazosulfuron-ethyl.

    PubMed

    Yun, M S; Shim, I S; Usui, K

    2001-03-01

    To investigate the selectivity and safening action of the sulfonylurea herbicide pyrazosulfuron-ethyl (PSE), pyrazosulfuron-ethyl O-demethylase (PSEOD) activity involving oxidative metabolism by cytochrome P-450 was studied in rice (Oryza sativa L cv Nipponbare) and Cyperus serotinus Rottb. Cytochrome P-450-dependent activity was demonstrated by the use of the inducers 1,8-naphthalic anhydride and ethanol, the herbicides PSE, bensulfuron-methyl, dimepiperate and dymron, or the inhibitor piperonyl butoxide (PBO). Growth inhibition in C serotinus seedlings was more severe than that in rice seedlings. O-Dealkylation activities of PSE were induced differently in rice and in C serotinus, with distinctly higher activity in rice seedlings. The induced PSEOD activities were slightly inhibited by PBO in rice seedlings, whereas they were strongly inhibited in C serotinus seedlings. Dimepiperate and dymron were effective safeners of rice against PSE treatment. Treatments with herbicide alone resulted in less induction of PSEOD activity compared with combined treatments of the herbicide and safener. PSEOD activity in rice seedlings induced with herbicide alone was strongly inhibited by PBO, whereas it was weakly inhibited in rice seedlings induced with combinations of PSE and two safeners. These results suggest that O-demethylation by cytochrome P-450 enzymes may be involved in the metabolism of PSE and may contribute to its selectivity and safening action. Furthermore, these results suggest the existence of a multiple form of cytochrome P-450 in plants.

  15. Balance of activities of alcohol acetyltransferase and esterase in Saccharomyces cerevisiae is important for production of isoamyl acetate.

    PubMed

    Fukuda, K; Yamamoto, N; Kiyokawa, Y; Yanagiuchi, T; Wakai, Y; Kitamoto, K; Inoue, Y; Kimura, A

    1998-10-01

    Isoamyl acetate is synthesized from isoamyl alcohol and acetyl coenzyme A by alcohol acetyltransferase (AATFase) in Saccharomyces cerevisiae and is hydrolyzed by esterases at the same time. We hypothesized that the balance of both enzyme activities was important for optimum production of isoamyl acetate in sake brewing. To test this hypothesis, we constructed yeast strains with different numbers of copies of the AATFase gene (ATF1) and the isoamyl acetate-hydrolyzing esterase gene (IAH1) and used these strains in small-scale sake brewing. Fermentation profiles as well as components of the resulting sake were largely alike; however, the amount of isoamyl acetate in the sake increased with an increasing ratio of AATFase/Iah1p esterase activity. Therefore, we conclude that the balance of these two enzyme activities is important for isoamyl acetate accumulation in sake mash.

  16. Balance of Activities of Alcohol Acetyltransferase and Esterase in Saccharomyces cerevisiae Is Important for Production of Isoamyl Acetate

    PubMed Central

    Fukuda, Kiyoshi; Yamamoto, Nagi; Kiyokawa, Yoshifumi; Yanagiuchi, Toshiyasu; Wakai, Yoshinori; Kitamoto, Katsuhiko; Inoue, Yoshiharu; Kimura, Akira

    1998-01-01

    Isoamyl acetate is synthesized from isoamyl alcohol and acetyl coenzyme A by alcohol acetyltransferase (AATFase) in Saccharomyces cerevisiae and is hydrolyzed by esterases at the same time. We hypothesized that the balance of both enzyme activities was important for optimum production of isoamyl acetate in sake brewing. To test this hypothesis, we constructed yeast strains with different numbers of copies of the AATFase gene (ATF1) and the isoamyl acetate-hydrolyzing esterase gene (IAH1) and used these strains in small-scale sake brewing. Fermentation profiles as well as components of the resulting sake were largely alike; however, the amount of isoamyl acetate in the sake increased with an increasing ratio of AATFase/Iah1p esterase activity. Therefore, we conclude that the balance of these two enzyme activities is important for isoamyl acetate accumulation in sake mash. PMID:9758847

  17. Computer Aided Prediction of Biological Activity Spectra: Study of Correlation between Predicted and Observed Activities for Coumarin-4-Acetic Acids

    PubMed Central

    Basanagouda, M.; Jadhav, V. B.; Kulkarni, M. V.; Rao, R. Nagendra

    2011-01-01

    Coumarin-4-acetic acids have been synthesized from various phenols and citric acid under Pechmann cyclisation conditions. All the compounds have been evaluated for antiinflammatory and analgesic activity in acute models. Compounds have also been evaluated for their ulcerogenic potential. Using the computer program, prediction of activity spectra for substances, prediction results and their Pharma Expert software, we have found a correlation between the observed and predicted antiinflammatory activity. PMID:22131629

  18. Ethyl ether

    Integrated Risk Information System (IRIS)

    Ethyl ether ; CASRN 60 - 29 - 7 Human health assessment information on a chemical substance is included in the IRIS database only after a comprehensive review of toxicity data , as outlined in the IRIS assessment development process . Sections I ( Health Hazard Assessments for Noncarcinogenic Effect

  19. Ethyl carbamate

    Integrated Risk Information System (IRIS)

    Ethyl carbamate ; CASRN 51 - 79 - 6 Human health assessment information on a chemical substance is included in the IRIS database only after a comprehensive review of toxicity data , as outlined in the IRIS assessment development process . Sections I ( Health Hazard Assessments for Noncarcinogenic Ef

  20. Ethyl chloride

    Integrated Risk Information System (IRIS)

    Ethyl chloride ; CASRN 75 - 00 - 3 Human health assessment information on a chemical substance is included in the IRIS database only after a comprehensive review of toxicity data , as outlined in the IRIS assessment development process . Sections I ( Health Hazard Assessments for Noncarcinogenic Eff

  1. Studies on antimicrobial activity of Poncirus trifoliata ethyl extract fraction against methicillin-resistant Staphylococcus aureus and to elucidate its antibacterial mechanism.

    PubMed

    Eom, Sung-Hwan; Jung, Yeoun-Joong; Lee, Dae-Sung; Yim, Mi-Jin; Kim, Hye Seon; Lee, Sang-Hoon; Myeong, Jeong-In; Lee, Jinhwan; Kim, Hyun-Woo; Kim, Kyoung-Ho; Lee, Myung-Suk; Kim, Young-Mog

    2016-01-01

    Traditional medicinal plants contain a wide variety of chemicals that have potent antibacterial activity. To find an alternative agent of overcoming the problems of methicillin-resistant Staphylococcus aureus (MRSA), the antibacterial mechanism of Ponciruss trifoliata against MRSA was investigated. Ethyl acetate (EtOAc)-soluble extract of P. trifoliata methanolic extract was evaluated for antibacterial activity using minimum inhibitory concentration (MIC). An EtOAc sub-fraction 08 (EA08) from silica-gel open column chromatography exhibited strong anti-MRSA activity. Apart from the study to isolate single compound from EA08, a synergistic antibacterial effect between the sub-fraction and β-lactam antibiotics against MRSA was determined. In order to elucidate the antibacterial restoring mechanism of EA08 on MRSA, mRNA expression of mecA gene and production penicillin-binding protein 2a (PBP2a) encoded by mecA gene were monitored. EA 08 showed the strongest antibacterial activity with MIC value of 256 μg ml(-1). MIC of oxacillin against MRSA was dramatically reduced from 512 to 16 μg ml(-1) in combination with 256 μg ml(-1) of EA08. The fractional inhibitory concentration index of oxacillin was measured at 0.53 in combination with EA08 against MRSA, suggesting that EA08-oxacillin combinations exert synergetic effect against MRSA. The analysis of RT-PCR and Western blotting profiles revealed that EA08 inhibited mRNA expression of mecA gene and production PBP2a, which is a key determinant for β-lactam antibiotic resistance, in a dose-dependent manner. These results indicated that EA08 eventually led to the reduction or inhibition of PBP2a production through translational inhibition in MRSA.

  2. Acetate as an active metabolite of ethanol: studies of locomotion, loss of righting reflex, and anxiety in rodents.

    PubMed

    Pardo, Marta; Betz, Adrienne J; San Miguel, Noemí; López-Cruz, Laura; Salamone, John D; Correa, Mercè

    2013-01-01

    IT HAS BEEN POSTULATED THAT A NUMBER OF THE CENTRAL EFFECTS OF ETHANOL ARE MEDIATED VIA ETHANOL METABOLITES: acetaldehyde and acetate. Ethanol is known to produce a large variety of behavioral actions such anxiolysis, narcosis, and modulation of locomotion. Acetaldehyde contributes to some of those effects although the contribution of acetate is less known. In the present studies, rats and mice were used to assess the acute and chronic effects of acetate after central or peripheral administration. Male Sprague-Dawley rats were used for the comparison between central (intraventricular, ICV) and peripheral (intraperitoneal, IP) administration of acute doses of acetate on locomotion. CD1 male mice were used to study acute IP effects of acetate on locomotion, and also the effects of chronic oral consumption of acetate (0, 500, or 1000 mg/l, during 7, 15, 30, or 60 days) on ethanol- (1.0, 2.0, 4.0, or 4.5 g/kg, IP) induced locomotion, anxiolysis, and loss of righting reflex (LORR). In rats, ICV acetate (0.7-2.8 μmoles) reduced spontaneous locomotion at doses that, in the case of ethanol and acetaldehyde, had previously been shown to stimulate locomotion. Peripheral acute administration of acetate also suppressed locomotion in rats (25-100 mg/kg), but not in mice. In addition, although chronic administration of acetate during 15 days did not have an effect on spontaneous locomotion in an open field, it blocked ethanol-induced locomotion. However, ethanol-induced anxiolysis was not affected by chronic administration of acetate. Chronic consumption of acetate (up to 60 days) did not have an effect on latency to, or duration of LORR induced by ethanol, but significantly increased the number of mice that did not achieve LORR. The present work provides new evidence supporting the hypothesis that acetate should be considered a centrally-active metabolite of ethanol that contributes to some behavioral effects of this alcohol, such as motor suppression.

  3. Effect of Pd surface structure on the activation of methyl acetate

    SciTech Connect

    Xu, Lijun; Xu, Ye

    2011-01-01

    The activation of methyl acetate (CH3COOCH3; MA) has been studied using periodic density functional theory calculations to probe the effect of Pd surface structure on the selectivity in MA activation. The adsorption of MA, dehydrogenated derivatives, enolate (CH2COOCH3; ENL) and methylene acetate (CH3COOCH2; MeA), and several dissociation products (including acetate, acetyl, ketene, methoxy, formaldehyde, CO, C, O, and H); and C-H and C-O (mainly in the RCO-OR position) bond dissociation in MA, ENL, and MeA, are calculated on Pd(111) terrace, step, and kink; and on Pd(100) terrace and step. The adsorption of most species is not strongly affected between (111)- to (100)-type surfaces, but is clearly enhanced by step/kink compared to the corresponding terrace. Going from terrace to step edge and from (111)- to (100)-type surfaces both stabilize the transition states of C-O bond dissociation steps. Going from terrace to step edge also stabilizes the transition states of C-H bond dissociation steps, but going from (111)- to (100)-type surfaces does not clearly do so. We propose that compared to the Pd(111) terrace, the Pd(100) terrace is more selective for C-O bond dissociation that is desirable for alcohol formation, whereas the Pd step edges are more selective for C-H bond dissociation.

  4. 27 CFR 21.107 - Ethyl acetate.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... by weight. (5) Specific gravity at 20 °/20 °C. Not less than 0.882. (6) Distillation range. (For.... (5) Specific gravity at 20 °/20 °C. Not less than 0.899. (6) Distillation range. (For applicable...

  5. 27 CFR 21.107 - Ethyl acetate.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... by weight. (5) Specific gravity at 20 °/20 °C. Not less than 0.882. (6) Distillation range. (For.... (5) Specific gravity at 20 °/20 °C. Not less than 0.899. (6) Distillation range. (For applicable...

  6. 27 CFR 21.107 - Ethyl acetate.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... by weight. (5) Specific gravity at 20 °/20 °C. Not less than 0.882. (6) Distillation range. (For.... (5) Specific gravity at 20 °/20 °C. Not less than 0.899. (6) Distillation range. (For applicable...

  7. 27 CFR 21.107 - Ethyl acetate.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... by weight. (5) Specific gravity at 20 °/20 °C. Not less than 0.882. (6) Distillation range. (For.... (5) Specific gravity at 20 °/20 °C. Not less than 0.899. (6) Distillation range. (For applicable...

  8. 27 CFR 21.107 - Ethyl acetate.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... by weight. (5) Specific gravity at 20 °/20 °C. Not less than 0.882. (6) Distillation range. (For.... (5) Specific gravity at 20 °/20 °C. Not less than 0.899. (6) Distillation range. (For applicable...

  9. Characteristics of Zinc Phosphate Coating Activated by Different Concentrations of Nickel Acetate Solution

    NASA Astrophysics Data System (ADS)

    Abdalla, Khalid; Zuhailawati, H.; Rahmat, Azmi; Azizan, A.

    2017-02-01

    Activation pretreatment with nickel acetate solution at various concentrations was performed prior to the phosphating step to enhance the corrosion resistance of carbon steel substrates. The activation solution was studied over various concentrations: 10, 50, and 100 g/L. The effects of these concentrations on surface characteristics and microstructural evolution of the coated samples were characterized by scanning electron microscopy and energy-dispersive spectroscopy. The electrochemical behavior was evaluated using potentiodynamic polarization curves, electrochemical impedance spectroscopy, and immersion test in a 3.5 pct NaCl solution. Significant increases in the nucleation sites and surface coverage of zinc phosphate coating were observed as the concentration of activation solution reached 50 g/L. The electrochemical analysis revealed that the activation treatment with 50 g/L nickel acetate solution significantly improved the protection ability of the zinc phosphate coating. The corrosion current density of activated phosphate coating with 50 g/L was reduced by 64.64 and 13.22 pct, compared to the coatings obtained with activation solutions of 10 and 100 g/L, respectively.

  10. Antiprotozoal, anticancer and antimicrobial activities of dihydroartemisinin acetal dimers and monomers

    PubMed Central

    Slade, Desmond; Galal, Ahmed M.; Gul, Waseem; Radwan, Mohamed M.; Ahmed, Safwat A.; Khan, Shabana I.; Tekwani, Babu L.; Jacob, Melissa R.; Ross, Samir A.; ElSohly, Mahmoud A.

    2009-01-01

    Nine dihydroartemisinin acetal dimers (6–14) with diversely functionalized linker units were synthesized and tested for in vitro antiprotozoal, anticancer and antimicrobial activity. Compounds 6, 7 and 11 [IC50: 3.0–6.7 nM (D6) and 4.2–5.9 nM (W2)] were appreciably more active than artemisinin (1) [IC50: 32.9 nM (D6) and 42.5 nM (W2)] against the chloroquine-sensitive (D6) and chloroquine-resistant (W2) strains of the malaria parasite, Plasmodium falciparum. Compounds 10, 13 and 14 displayed enhanced anticancer activity in a number of cell lines compared to the control drug, doxorubicin. The antifungal activity of 7 and 12 against Cryptococcus neoformans (IC50: 0.16 and 0.55 μM, respectively) was also higher compared to the control drug, amphotericin B. The antileishmanial and antibacterial activities were marginal. A number of dihydroartemisinin acetal monomers (15–17) and a trimer (18) were isolated as byproducts from the dimer synthesis and were also tested for biological activity. PMID:19879765

  11. Breeding of a sake yeast mutant with enhanced ethyl caproate productivity in sake brewing using rice milled at a high polishing ratio.

    PubMed

    Takahashi, Toshinari; Ohara, Yusuke; Sueno, Kazuo

    2017-03-09

    Sake yeast produces a fruity flavor known as ginjo-ko-which is mainly attributable to ethyl caproate and isoamyl acetate-during fermentation in sake brewing. The production of these flavor components is inhibited by unsaturated fatty acids derived from the outer layer of rice as raw material. We isolated three mutants (hec2, hec3, and hec6) with enhanced ethyl caproate productivity in sake brewing using rice milled at a high polishing ratio from a cerulenin-resistant mutant derived from the hia1 strain, which shows enhanced isoamyl acetate productivity. The hec2 mutant had the homozygous FAS2 mutation Gly1250Ser, which is known to confer high ethyl caproate productivity. When the homozygous FAS2 mutation Gly1250Ser was introduced into strain hia1, ethyl caproate productivity was increased but neither this nor intracellular caproic acid content approached the levels observed in the hec2 mutant, indicating that a novel mutation was responsible for the high ethyl caproate productivity. We also found that the expression of EEB1 encoding acyl-coenzyme A: ethanol O-acyltransferase (AEATase) and enzymatic activity were increased in the hec2 mutant. These results suggest that the upregulation of EEB1 expression and AEATase activity may also have contributed to the enhancement of ethyl caproate synthesis from ethanol and caproyl-CoA. Our findings are useful for the brewing of sake with improved flavor due to high levels of isoamyl acetate and ethyl caproate.

  12. Design, synthesis, and calcium channel antagonist activity of new 1,4-dihydropyridines containing 4-(5)-chloro-2-ethyl-5-(4)-imidazolyl substituent.

    PubMed

    Davood, Asghar; Mansouri, Niloufar; Rerza Dehpour, Ahmad; Shafaroudi, Hamed; Alipour, Eskandar; Shafiee, Abbas

    2006-06-01

    A series of dialkyl, dicycloalkyl, and diaryl ester analogues of nifedipine, in which the ortho-nitro phenyl group at position 4 is replaced by the 4-(5)-chloro-2-ethyl-5-(4)-imidazolyl substituent, were synthesized and evaluated as calcium channel antagonists using the high K+ contraction of guinea pig ileal longitudinal smooth muscle. The results for the symmetrical ester series showed that increasing the length of the chain in C3- and C5-ester substituents increased the activity and the most active compound was the diphenylethyl ester derivative, so it was more active than the reference drug nifedipine. In unsymmetrical diester series, when R1 is methyl or ethyl, increasing lipophilic properties in the R substituent, increased the activity. The most active compounds were methyl/phenethyl and ethyl/phenethyl ester derivatives, being slightly more active than nifedipine.

  13. Crystal structure of ethyl 2-[9-(5-bromo-2-hy­droxy­phen­yl)-1,8-dioxo-1,2,3,4,5,6,7,8,9,10-deca­hydro­acridin-10-yl]acetate

    PubMed Central

    Mohamed, Shaaban K.; Akkurt, Mehmet; Jasinski, Jerry P.; Abdelhamid, Antar A.; Tamam, Asmaa H.; Albayati, Mustafa R.

    2015-01-01

    In the title compound, C23H24BrNO5, the central 1,4-di­hydro­pyridine ring of the 1,2,3,4,5,6,7,8,9,10-deca­hydro­acridine ring system adopts a half-chair conformation. The two cyclo­hexene rings fused to the central ring both have a twisted-boat conformation. The mean planes of the bromo­hydroxy­phenyl ring and the major and minor components of the disordered ethyl amino­acetate moiety make dihedral angles of 78.99 (12), 85.9 (2) and 88.3 (9)°, respectively, with the 1,4-di­hydro­pyridine ring. The terminal ethyl group of the ethyl amino­acetate moiety is disordered over two sets of sites with refined occupancies of 0.768 (17) and 0.232 (17). The mol­ecular conformation is stabilized by an intra­molecular O—H⋯O hydrogen bond, forming an S(8) ring motif. In the crystal, C—H⋯O hydrogen bonds connect the mol­ecules into layers parallel to (001), enclosing R 1 2(7) ring motifs. PMID:26870566

  14. Novel N-2-(Furyl)-2-(chlorobenzyloxyimino) Ethyl Piperazinyl Quinolones: Synthesis, Cytotoxic Evaluation and Structure-Activity Relationship

    PubMed Central

    Mohammadhosseini, Negar; Pordeli, Mahboobeh; Safavi, Maliheh; Firoozpour, Loghman; Amin, Fatame; Kabudanian Ardestani, Sussan; Edraki, Najmeh; Shafiee, Abbas; Foroumadi, Alireza

    2015-01-01

    Quinolone antibacterials are one of the most important classes of pharmacological agents known as potent inhibitors of bacterial DNA gyrase and topoisomerase IV that efficiently inhibit DNA replication and transcription by generating several double-stranded DNA break. Some quinolone derivatives demonstrated inhibitory potential against eukaryote topoismarase II and substantial dose-dependent cytotoxic potential against some cancerous cells. In present study, synthesis and cytotoxic activity evaluation of new series of N-pipearzinyl quinolones containing N-2-(furyl-2 or 3-yl)-2-(chlorobenzyloxyimino) ethyl moiety 7a-i have been studied. Reaction of quinolone, with 2-bromo-1-(furan-2 or 3-yl)ethanone-O-substituted chlorobenzyloxime in DMF in presence of NaHCO3 at room temperature, gave the title compounds N-2-(furan-2 or 3-yl)-2-(chlorobenzyloxyiminoethyl) quinolone 7a-i. Synthesized compounds were further evaluated in-vitro against three human breast tumor cell lines. Preliminary screening indicated that compound 7 g demonstrated significant growth inhibitory potential against all evaluated cell lines. The results of structure-activity relationship study exhibited that quinolone derivatives are superior in cytotoxic potential compared to 1, 8-naphthyridone series. Furthermore, ethyl quinolone derivatives were more potent cytotoxic agents comparing with cyclopropyl quinolones. PMID:26664376

  15. Acetate metabolism does not reflect astrocytic activity, contributes directly to GABA synthesis, and is increased by silent information regulator 1 activation.

    PubMed

    Rowlands, Benjamin D; Klugmann, Matthias; Rae, Caroline D

    2017-03-01

    [(13) C]Acetate is known to label metabolites preferentially in astrocytes rather than neurons and it has consequently been used as a marker for astrocytic activity. Recent discoveries suggest that control of acetate metabolism and its contributions to the synthesis of metabolites in brain is not as simple as first thought. Here, using a Guinea pig brain cortical tissue slice model metabolizing [1-(13) C]D-glucose and [1,2-(13) C]acetate, we investigated control of acetate metabolism and the degree to which it reflects astrocytic activity. Using a range of [1,2-(13) C]acetate concentrations, we found that acetate is a poor substrate for metabolism and will inhibit metabolism of itself and of glucose at concentrations in excess of 2 mmol/L. By activating astrocytes using potassium depolarization, we found that use of [1,2-(13) C]acetate to synthesize glutamine decreases significantly under these conditions showing that acetate metabolism does not necessarily reflect astrocytic activity. By blocking synthesis of glutamine using methionine sulfoximine, we found that significant amount of [1,2-(13) C]acetate are still incorporated into GABA and its metabolic precursors in neurons, with around 30% of the GABA synthesized from [1,2-(13) C]acetate likely to be made directly in neurons rather than from glutamine supplied by astrocytes. Finally, to test whether activity of the acetate metabolizing enzyme acetyl-CoA synthetase is under acetylation control in the brain, we incubated slices with the AceCS1 deacetylase silent information regulator 1 (SIRT1) activator SRT 1720 and showed consequential increased incorporation of [1,2-(13) C]acetate into metabolites. Taken together, these data show that acetate metabolism is not directly nor exclusively related to astrocytic metabolic activity, that use of acetate is related to enzyme acetylation and that acetate is directly metabolized to a significant degree in GABAergic neurons. Changes in acetate metabolism should be

  16. Adsorptive removal of phthalate ester (Di-ethyl phthalate) from aqueous phase by activated carbon: a kinetic study.

    PubMed

    Venkata Mohan, S; Shailaja, S; Rama Krishna, M; Sarma, P N

    2007-07-19

    Adsorptive studies were carried out on Di-ethyl phthalate (DEP) removal from aqueous phase onto activated carbon. Batch sorption studies were performed and the results revealed that activated carbon demonstrated ability to adsorb DEP. Influence of varying experimental conditions such as DEP concentration, pH of aqueous solution, and dosage of adsorbent were investigated on the adsorption process. Sorption interaction of DEP onto activated carbon obeyed the pseudo second order rate equation. Experimental data showed good fit with both the Langmuir and Freundlich adsorption isotherm models. DEP sorption was found to be dependent on the aqueous phase pH and the uptake was observed to be greater at acidic pH.

  17. Phase Preference by Active, Acetate-Utilizing Bacteria at the Rifle, CO Integrated Field Research Challenge Site

    SciTech Connect

    Kerkhof, L.; Williams, K.H.; Long, P.E.; McGuinness, L.

    2011-02-21

    Previous experiments at the Rifle, Colorado Integrated Field Research Challenge (IFRC) site demonstrated that field-scale addition of acetate to groundwater reduced the ambient soluble uranium concentration. In this report, sediment samples collected before and after acetate field addition were used to assess the active microbes via {sup 13}C acetate stable isotope probing on 3 phases [coarse sand, fines (8-approximately 150 {micro}m), groundwater (0.2-8 {micro}m)] over a 24-day time frame. TRFLP results generally indicated a stronger signal in {sup 13}C-DNA in the 'fines' fraction compared to the sand and groundwater. Before the field-scale acetate addition, a Geobacter-like group primarily synthesized {sup 13}C-DNA in the groundwater phase, an alpha Proteobacterium primarily grew on the fines/sands, and an Acinetobacter sp. and Decholoromonas-like OTU utilized much of the {sup 13}C acetate in both groundwater and particle-associated phases. At the termination of the field-scale acetate addition, the Geobacter-like species was active on the solid phases rather than the groundwater, while the other bacterial groups had very reduced newly synthesized DNA signal. These findings will help to delineate the acetate utilization patterns of bacteria in the field and can lead to improved methods for stimulating distinct microbial populations in situ.

  18. Enhancement of acetyl xylan esterase activity on cellulose acetate through fusion to a family 3 cellulose binding module.

    PubMed

    Mai-Gisondi, Galina; Turunen, Ossi; Pastinen, Ossi; Pahimanolis, Nikolaos; Master, Emma R

    2015-11-01

    The current study investigates the potential to increase the activity of a family 1 carbohydrate esterase on cellulose acetate through fusion to a family 3 carbohydrate binding module (CBM). Specifically, CtCBM3 from Clostridium thermocellum was fused to the carboxyl terminus of the acetyl xylan esterase (AnAXE) from Aspergillus nidulans, and active forms of both AnAXE and AnAXE-CtCBM3 were produced in Pichia pastoris. CtCBM3 fusion had negligible impact on the thermostability or regioselectivity of AnAXE; activities towards acetylated corncob xylan, 4-methylumbelliferyl acetate, p-nitrophenyl acetate, and cellobiose octaacetate were also unchanged. By contrast, the activity of AnAXE-CtCBM3 on cellulose acetate increased by two to four times over 24 h, with greater differences observed at earlier time points. Binding studies using microcrystalline cellulose (Avicel) and a commercial source of cellulose acetate confirmed functional production of the CtCBM3 domain; affinity gel electrophoresis using acetylated xylan also verified the selectivity of CtCBM3 binding to cellulose. Notably, gains in enzyme activity on cellulose acetate appeared to exceed gains in substrate binding, suggesting that fusion to CtCBM3 increases functional associations between the enzyme and insoluble, high molecular weight cellulosic substrates.

  19. Reactivity and regioselectivity in reactions of methyl and ethyl azides with cyclooctynes: activation strain model and energy decomposition analysis.

    PubMed

    de S Vilhena, Felipe; de M Carneiro, José Walkimar

    2017-01-01

    The structures and energies for the Huisgen 1,3-dipolar cycloaddition reactions of methyl and ethyl azides with some cyclooctynes and dibenzocyclooctynes were computed at the B3LYP/6-311++G(d,p) level. The activation strain model (ASM) and quantitative molecular orbital (MO) theory were used to investigate the reactivity and regiochemistry in these reactions. The energy decomposition analysis (EDA) was used to identify the intrinsic electronic factor that lead to the preferential formation of 1,7-regiochemistry products. The reactivity order agrees with formation of more synchronous transition states and lower distortion energies. For the reaction of N3Met with azacyclooctyne, the 1,7-regiochemistry preference is attributed to a lower FMO gap and a higher contribution of the polarization term of the interaction energy than for the 1,8-transition state. For the reaction with aza-dibenzocyclooctyne, the 1,7-preference is due to a lower strain energy and a more pronounced contribution of the exchange term of the interaction energy. Graphical Abstract In the reactions between methyl and ethyl azides with azacyclooctynes the regiochemistry is governed by the intrinsic electronic factors.

  20. Regulation of astrocyte activity via control over stiffness of cellulose acetate electrospun nanofiber.

    PubMed

    Min, Seul Ki; Jung, Sang Myung; Ju, Jung Hyeon; Kwon, Yeo Seon; Yoon, Gwang Heum; Shin, Hwa Sung

    2015-10-01

    Astrocytes are involved in neuron protection following central nervous system (CNS) injury; accordingly, engineered astrocytes have been investigated for their usefulness in cell therapy for CNS injury. Nanofibers have attracted a great deal of attention in neural tissue engineering, but their mechanical properties greatly influence physiology. Cellulose acetate (CA) has been studied for use in scaffolds owing to its biocompatibility, biodegradability, and good thermal stability. In this study, stiffness of CA nanofibers controlled by heat treatment was shown to regulate astrocyte activity. Adhesion and viability increased in culture as substrate became stiffer but showed saturation at greater than 2 MPa of tensile strength. Astrocytes became more active in terms of increasing intermediate filament glial fibrillary acidic protein (GFAP). The results of this study demonstrate the effects of stiffness alone on cellular behaviors in a three-dimensional culture and highlight the efficacy of heat-treated CA for astrocyte culture in that the simple treatment enables control of astrocyte activity.

  1. Phase Preference by Active, Acetate-Utilizing Bacteria at the Rifle, CO Integrated Field Research Challenge Site

    SciTech Connect

    Kerkhoff, Lee; Williams, Kenneth H.; Long, Philip E.; McGuinness, L.

    2011-02-15

    Uranium contaminated groundwaters are a legacy concern for the U.S. Department of Energy. Previous experiments at the Rifle, Colorado Integrated Field Challenge (IFC) site have demonstrated that field-scale addition of acetate to groundwater reduces the ambient soluable uranium concentration, sequestering the radionuclide as uraninite. However, questions remain regarding which microorganism(s) are consuming this acetate and if active groundwater microorganisms are different from active particle-associated bacteria. In this report, 13-C acetate was used to assess the active microbes that synthesize DNA on 3 size fractions [coarse sand, fines (8-approximately 150 micron), groundwater (0.2-8 micron)] over a 24 -day time frame. Results indicated a stronger signal from 13-C acetate associated with the “fines” fraction compared with smaller amounts of 13-C uptake on the sand fraction and groundwater samples during the SIP incubations. TRFLP analysis of this 13-C-labeled DNA, indicated 31+ 9 OTU's with 6 peaks dominating the active profiles (166, 187, 210, 212, and 277 bp peaks using MnlI). Cloning/sequencing of the amplification products indicated a Geobacter-like group (187, 210, 212 bp) primarily synthesized DNA from acetate in the groundwater phase, an alpha Proteobacterium (166 bp) primarily grew on the fines/sands, and an Acinetobacter sp. (277 bp) utilized much of the 13C acetate in both groundwater and particle-associated phases. These findings will help to delineate the acetate utilization patterns of bacteria during field-scale acetate addition and can lead to improved methods for stimulating distinct microbial populations in situ.

  2. Sodium acetate inhibits Staphylococcus aureus internalization into bovine mammary epithelial cells by inhibiting NF-κB activation.

    PubMed

    Wei, Zhengkai; Xiao, Chong; Guo, Changming; Zhang, Xu; Wang, Yanan; Wang, Jingjing; Yang, Zhengtao; Fu, Yunhe

    2017-03-27

    Bovine mastitis is one of the most costly and prevalent disease affecting dairy cows worldwide. It was reported that Staphylococcus aureus could internalize into bovine mammary epithelial cells (bMEC) and induce mastitis. Some short chain fatty acids (SCFA) have shown to suppress S. aureus invasion into bMEC and regulate antimicrobial peptides expression. But it has not been evaluated that sodium acetate has the similar effect. The aim of this study was to investigate the effect of sodium acetate on the invasion of bovine mammary epithelial cells (bMEC) by S. aureus. Gentamicin protection assay showed that the invasion of S. aureus into bMEC was inhibited by sodium acetate in a dose-dependent manner. Sodium acetate (0.25-5 mM) did not affect S. aureus growth and bMEC viability. The TAP gene level was decreased, while the BNBD5 mRNA level was enhanced in sodium acetate treated bMEC. In sodium acetate treated and S. aureus challenged bMEC, the TAP gene expression was increased and BNBD5 gene expression was not modified at low concentrations, but decreased at high concentrations. The Nitric oxide (NO) production of bMEC after S. aureus stimulation was decreased by sodium acetate treatment. Furthermore, sodium acetate treatment suppressed S. aureus-induced NF-κB activation in bMEC in a dose manner. In conclusion, our results suggested that sodium acetate exerts an inhibitory property on S. aureus internalization and modulates antimicrobial peptides gene expression.

  3. Synthesis and antiviral activity of the carbocyclic analogues of 5-ethyl-2'-deoxyuridine and of 5-ethynyl-2'-deoxyuridine.

    PubMed

    Shealy, Y F; O'Dell, C A; Arnett, G; Shannon, W M

    1986-01-01

    The carbocyclic analogue of the antiviral agent 5-ethyl-2'-deoxyuridine (EDU) was synthesized by two routes. The pivotal step in the first route is the reaction of lithium dimethylcuprate with the carbocyclic analogue of 5-(bromomethyl)-2'-deoxyuridine dibenzoate (6). The second route is based on the synthesis of the carbocyclic analogue of 5-ethynyl-2'-deoxyuridine (12) by a coupling reaction catalyzed by bis(triphenylphosphine)palladium(II) chloride and copper(I) iodide, a method reported recently (Robins and Barr) for the synthesis of the true nucleoside 5-ethynyl-2'-deoxyuridine (1b). The carbocyclic analogue of EDU inhibits the replication of type 1 and type 2 herpes simplex viruses in Vero cells. The carbocyclic analogue of 5-ethynyl-2'-deoxyuridine has modest activity against herpes simplex virus, types 1 and 2.

  4. Effect of agitation on removal of acetic acid from pretreated hydrolysate by activated carbon.

    PubMed

    Priddy, Sarah A; Hanley, Thomas R

    2003-01-01

    The effect of agitation on the adsorption of acetic acid by activated carbon was tested utilizing an external mass transfer-diffusion model. Simulated pretreated biomass was contacted with activated carbon under prescribed conditions of temperature and agitation. Adsorption isotherm studies are presented as well as batch kinetic rate studies. Use of these data enabled the determination of isotherm constants, an external mass transfer coefficient, and an effective diffusivity for each agitation rate studied. The external film coefficient results ranged from 33.62 microm/s to a complete absence of external mass transfer resistance, and the diffusivity results ranged from 0.8625 to 10.70 microm(2)/s. The optimum combination of no external film resistance, and highest diffusivity, 10.70 microm(2)/s, occurred at 250 rpm and 25 degrees C. The results of these models and the experimental parameters suggested an efficacious method and conditions for the removal of this undesirable chemical.

  5. Enhanced Activity of Nanocrystalline Beta Zeolite for Acylation of Veratrole with Acetic Anhydride.

    PubMed

    Aisha Mahmood Abdulkareem, Al-Turkustani; Selvin, Rosilda

    2016-04-01

    Friedel-Craft acylation of veratrole using homogeneous acid catalysts such as AlCl3, FeCl3, ZnCl2, and HF etc. produces acetoveratrone, (3',4'-dimethoxyacetophenone), which is the intermediate for synthesis of papavarine alkaloids. The problems associated with these homogeneous catalysts can be overcome by using heterogeneous solid catalysts. Since acetoveratrone is a larger molecule, large pore Beta zeolites with smaller particle sizes are beneficial for the liquid-phase acylation of veratrole, for easy diffusion of reactants and products. The present study aims in the acylation of veratrole with acetic anhydride using nanocrystalline Beta Zeolite catalyst. A systematic investigation of the effects of various reaction parameters was done. The catalysts were characterized for their structural features by using XRD, TEM and DLS analyses. The catalytic activity of nanocrystalline Beta zeolite was compared with commercial Beta zeolite for the acylation and was found that nanocrystalline Beta zeolite possessed superior activity.

  6. Acetate as an active metabolite of ethanol: studies of locomotion, loss of righting reflex, and anxiety in rodents

    PubMed Central

    Pardo, Marta; Betz, Adrienne J.; San Miguel, Noemí; López-Cruz, Laura; Salamone, John D.; Correa, Mercè

    2013-01-01

    It has been postulated that a number of the central effects of ethanol are mediated via ethanol metabolites: acetaldehyde and acetate. Ethanol is known to produce a large variety of behavioral actions such anxiolysis, narcosis, and modulation of locomotion. Acetaldehyde contributes to some of those effects although the contribution of acetate is less known. In the present studies, rats and mice were used to assess the acute and chronic effects of acetate after central or peripheral administration. Male Sprague-Dawley rats were used for the comparison between central (intraventricular, ICV) and peripheral (intraperitoneal, IP) administration of acute doses of acetate on locomotion. CD1 male mice were used to study acute IP effects of acetate on locomotion, and also the effects of chronic oral consumption of acetate (0, 500, or 1000 mg/l, during 7, 15, 30, or 60 days) on ethanol- (1.0, 2.0, 4.0, or 4.5 g/kg, IP) induced locomotion, anxiolysis, and loss of righting reflex (LORR). In rats, ICV acetate (0.7–2.8 μmoles) reduced spontaneous locomotion at doses that, in the case of ethanol and acetaldehyde, had previously been shown to stimulate locomotion. Peripheral acute administration of acetate also suppressed locomotion in rats (25–100 mg/kg), but not in mice. In addition, although chronic administration of acetate during 15 days did not have an effect on spontaneous locomotion in an open field, it blocked ethanol-induced locomotion. However, ethanol-induced anxiolysis was not affected by chronic administration of acetate. Chronic consumption of acetate (up to 60 days) did not have an effect on latency to, or duration of LORR induced by ethanol, but significantly increased the number of mice that did not achieve LORR. The present work provides new evidence supporting the hypothesis that acetate should be considered a centrally-active metabolite of ethanol that contributes to some behavioral effects of this alcohol, such as motor suppression. PMID:23847487

  7. CHARACTERIZATION ADN BIOLOGICAL ACTIVITY OF SECONDARY METABOLITES FROM ARMILLARIA TABESCENS

    Technology Transfer Automated Retrieval System (TEKTRAN)

    Ethyl acetate extracts from liquid cultures of Armillaria tabescens showed good antimicrobial activity against Candida albicans, Cryptococcus neoformans, Escherichia coli and Mycobacterium intracellulare. Chemical analyses of extract constituents led to the isolation and identification of two new co...

  8. Nitric oxide radical scavenging active components from Phyllanthus emblica L.

    PubMed

    Kumaran, A; Karunakaran, R Joel

    2006-03-01

    An activity-directed fractionation and purification process was used to identify the nitric oxide (NO) scavenging components of Phyllanthus emblica. Dried fruit rind of P. emblica was extracted with methanol and then separated into hexane, ethyl acetate, and water fractions. Among these only the ethyl acetate phase showed strong NO scavenging activity in vitro, when compared with water and hexane phases. The ethyl acetate fraction was then subjected to separation and purification using Sephadex LH-20 chromatography. Five compounds showing strong NO scavenging activity were identified by spectral methods (1H NMR, 13C NMR, and MS) and by comparison with literature values to be Gallic acid, Methyl gallate, Corilagin, Furosin, and Geraniin. In addition, HPLC identification and quantification of isolated compounds were also performed. Gallic acid was found to be a major compound in the ethyl acetate extract and Geraniin showed highest NO scavenging activity among the isolated compounds.

  9. Incensole acetate, an incense component, elicits psychoactivity by activating TRPV3 channels in the brain

    PubMed Central

    Moussaieff, Arieh; Rimmerman, Neta; Bregman, Tatiana; Straiker, Alex; Felder, Christian C.; Shoham, Shai; Kashman, Yoel; Huang, Susan M.; Lee, Hyosang; Shohami, Esther; Mackie, Ken; Caterina, Michael J.; Walker, J. Michael; Fride, Ester; Mechoulam, Raphael

    2008-01-01

    Burning of Boswellia resin as incense has been part of religious and cultural ceremonies for millennia and is believed to contribute to the spiritual exaltation associated with such events. Transient receptor potential vanilloid (TRPV) 3 is an ion channel implicated in the perception of warmth in the skin. TRPV3 mRNA has also been found in neurons throughout the brain; however, the role of TRPV3 channels there remains unknown. Here we show that incensole acetate (IA), a Boswellia resin constituent, is a potent TRPV3 agonist that causes anxiolytic-like and antidepressive-like behavioral effects in wild-type (WT) mice with concomitant changes in c-Fos activation in the brain. These behavioral effects were not noted in TRPV3−/− mice, suggesting that they are mediated via TRPV3 channels. IA activated TRPV3 channels stably expressed in HEK293 cells and in keratinocytes from TRPV3+/+ mice. It had no effect on keratinocytes from TRPV3−/− mice and showed modest or no effect on TRPV1, TRPV2, and TRPV4, as well as on 24 other receptors, ion channels, and transport proteins. Our results imply that TRPV3 channels in the brain may play a role in emotional regulation. Furthermore, the biochemical and pharmacological effects of IA may provide a biological basis for deeply rooted cultural and religious traditions.—Moussaieff, A., Rimmerman, N., Bregman, T., Straiker, A., Felder, C. C., Shoham, S., Kashman, Y., Huang, S. M., Lee, H., Shohami, E., Mackie, K., Caterina, M. J., Walker, J. M., Fride, E., Mechoulam, R. Incensole acetate, an incense component, elicits psychoactivity by activating TRPV3 channels in the brain. PMID:18492727

  10. In vitro antiproliferative and apoptosis-inducing activities of crude ethyle alcohole extract of Quercus brantii L. acorn and subsequent fractions.

    PubMed

    Moradi, Mohammad-Taghi; Karimi, Ali; Alidadi, Somayeh

    2016-03-01

    Cancer cell resistance to widely used chemotherapeutic agents is gradually developed. Natural products, mainly isolated from medicinal plants, have been considered as valuable sources for herbal anticancer drugs. The present study aimed to evaluate in vitro antiproliferative and apoptosis-inducing activities of crude ethyle alcohole extract and four fractions of Q. brantii acorn. Crude ethyle alcohole extract of Q. brantii acorn was prepared and subjected to fractionation with different polarity. Subsequently, the extract and the fractions wereevaluated for their in vitro antiproliferative activity in two cancerous (Hela and AGS) and one normal (HDFs) cell lines using MTT [3-(4, 5-dimethylthiazol-2ol) 2, 5 diphenyltetrazoliumbromide] assay. To determine whether the cytotoxicity of these compounds involved the induction of apoptosis, Hela cells were treated with IC50 concentrations of test compounds, stained with both propidium iodide (PI) and Annexin V-fluorescein isothiocyanate (FITC), and analyzed by flow cytometry. In vitro cytotoxicity assay showed that the cell viability was significantly reduced in a dose-dependent manner following treatment with crude ethyle alcohole extract and Cholophorm and n-Butanol fractions. Based on the probit regression model, antiproliferative activities of crude ethyle alcohole extract, Cholophorm fraction, and n-Butanol fraction on Hela and AGS cells and HDFs cells were significantly different (P < 0.001). The results of flow cytometric analysis showed that crude ethyle alcohole extract and two fractions of Q. brantii acorn induced early apoptotic cell death. These findings suggest that crude ethyle alcohole extract and Cholophorm and n-Butanol fractions of Q. brantii acorn suppress the proliferation of cancer cells through induction of early apoptosis.

  11. Anti-leukemic activity of Dillenia indica L. fruit extract and quantification of betulinic acid by HPLC.

    PubMed

    Kumar, Deepak; Mallick, Sumana; Vedasiromoni, Joseph R; Pal, Bikas C

    2010-05-01

    The methanolic extract of Dillenia indica L. fruits showed significant anti-leukemic activity in human leukemic cell lines U937, HL60 and K562. This finding led to fractionation of the methanolic extract, on the basis of polarity, in which the ethyl acetate fraction showed the highest anti-leukemic activity. A major compound, betulinic acid, was isolated from the ethyl acetate fraction by silica gel column chromatography and was identified and characterized. Betulinic acid could explain the anti-leukemic activity of the methanolic extract and the ethyl acetate fraction. Hence the quantitative estimation of betulinic acid was approached in methanolic extract and fractions using HPLC.

  12. Intestinal anti-inflammatory activity of calcium pyruvate in the TNBS model of rat colitis: Comparison with ethyl pyruvate.

    PubMed

    Algieri, F; Rodriguez-Nogales, A; Garrido-Mesa, J; Camuesco, D; Vezza, T; Garrido-Mesa, N; Utrilla, P; Rodriguez-Cabezas, M E; Pischel, I; Galvez, J

    2016-03-01

    Pyruvate is a key intermediate of the carbohydrate metabolism with endogenous scavenger properties. However, it cannot be used in clinics due to its instability. Ethyl pyruvate (EP) has shown better stability as well as an antioxidant and anti-inflammatory activity. Calcium pyruvate monohydrate (CPM) is another stable pyruvate derivative that could also provide the benefits from calcium, fundamental for bone health. Considering everything, we propose CPM as a therapeutic strategy to treat diseases with an immune component in which there is also a significant dysregulation of the skeletal homeostasis. This could be applicable to inflammatory bowel disease, which is characterized by over-production of pro-inflammatory mediators, including cytokines and reactive oxygen and nitrogen metabolites that induces intestinal mucosal damage and chronic inflammation, and extra-intestinal symptoms like osteopenia and osteoporosis. The effects of CPM and EP (20, 40 and 100mg/kg) were evaluated on the trinitrobenzenesulfonic acid (TNBS) model of colitis in rats, after a 7-day oral treatment, with main focus on colonic histology and inflammatory mediators. Both pyruvates showed intestinal anti-inflammatory effects in the TNBS-induced colitis. They were evident both histologically, with a recovery of the mucosal cytoarchitecture and a reduction of the neutrophil infiltration, and through the profile of inflammatory mediators (IL-1, IL-6, IL-17, IL-23, iNOS). However, CPM appeared to be more effective than ethyl pyruvate. In conclusion, CPM exerts intestinal anti-inflammatory effect on the TNBS-induced colitis in rats, although further experiments are needed to explore its beneficial effects on bone health and osteoporosis.

  13. Use of acetate for enrichment of electrochemically active microorganisms and their 16S rDNA analyses.

    PubMed

    Lee, Jiyoung; Phung, Nguyet Thu; Chang, In Seop; Kim, Byung Hong; Sung, Ha Chin

    2003-06-27

    A fuel cell-type electrochemical device has been used to enrich microbes oxidizing acetate with concomitant electricity generation without using an electron mediator from activated sludge. The device generated a stable current of around 5 mA with complete oxidation of 5 mM acetate at the hydraulic retention time of 2.5 h after 4 weeks of enrichment. Over 70% of electrons available from acetate oxidation was recovered as current. Carbon monoxide or hydrogen did not influence acetate oxidation or current generation from the microbial fuel cell (MFC). Denaturing gradient gel electrophoresis showed that DNA extracted from the acetate-enriched MFC had different 16S rDNA patterns from those of sludge or glucose+glutamate-enriched MFCs. Nearly complete 16S rDNA sequence analyses showed that diverse bacteria were enriched in the MFC fed with acetate. Electron microscopic observations showed biofilm developed on the electrode, but not microbial clumps observed in MFCs fed with complex fuel such as glucose and wastewater from a corn-processing factory.

  14. Rapid method for identification of macrophages in suspension by acid alpha-naphthyl acetate esterase activity.

    PubMed

    Ennist, D L; Jones, K H

    1983-07-01

    A supravital staining procedure for the identification of macrophages in cell suspension using a modification of a standard cytochemical assay for alpha-naphthyl acetate esterase (ANAE) activity is described. Macrophages are stained an intense red-brown after 5 min incubation in a buffer using ANAE as the substrate and hexazonium pararosaniline as the coupler for the azo dye. There is close agreement in the number of ANAE-positive cells found and the number of macrophages identified in smears by morphological criteria, by phagocytosis, and by the presence of Fc receptors. Therefore, this stain provides a quick, inexpensive method to estimate the number of macrophages present in suspensions of lymphocytic tissues from rats and mice.

  15. Synthesis, characterization and antibacterial activity of cellulose acetate-tin (IV) phosphate nanocomposite.

    PubMed

    Rathore, Bhim Singh; Sharma, Gaurav; Pathania, Deepak; Gupta, Vinod Kumar

    2014-03-15

    Cellulose acetate-tin (IV) phosphate nanocomposite (CA/TPNC) was prepared using simple method at 0-1 pH. The nanocomposite ion exchanger was characterized using some techniques such as Fourier transform infrared spectroscopy (FTIR), transmission electron microscopy (TEM), scanning electron microscopy (SEM), energy dispersive X-ray spectroscopy (EDX), X-ray diffraction (XRD), and thermogravimetric analysis (TGA/DTA/DSC). The nanocomposite material was explored for different properties such as ion exchange capacity, pH titration, elution behavior, thermal stability, and distribution coefficient. The ion exchange capacity of CA/TPNC was found higher compared to their inorganic counterpart. The distribution coefficient studies of nanocomposite ion exchanger were investigated for different metal ions. On the basis of distribution coefficient studies CA/TPNC material was found more selective for Cd(2+) and Mg(2+). CA/TPNC ion exchange was explored for antibacterial activities against E. coli bacteria.

  16. Ferulic acid ethyl ester diminished Complete Freund's Adjuvant-induced incapacitation through antioxidant and anti-inflammatory activity.

    PubMed

    Cunha, Francisco Valmor Macedo; Gomes, Bruno de Sousa; Neto, Benedito de Sousa; Ferreira, Alana Rodrigues; de Sousa, Damião Pergentino; de Carvalho e Martins, Maria do Carmo; Oliveira, Francisco de Assis

    2016-01-01

    Ferulic acid ethyl ester (FAEE) is a derivate from ferulic acid which reportedly has antioxidant effect; however, its role on inflammation was unknown. In this study, we investigated the orally administered FAEE anti-inflammatory activity on experimental inflammation models and Complete Freund's Adjuvant (CFA)-induced arthritis in rats. CFA-induced arthritis has been evaluated by incapacitation model and radiographic knee joint records at different observation time. FAEE (po) reduced carrageenan-induced paw edema (p < 0.001) within the 1st to 5th hours at 50 and 100 mg/kg doses. FAEE 50 and 100 mg/kg, po inhibited leukocyte migration into air pouch model (p < 0.001), and myeloperoxidase, superoxide dismutase, and catalase activities (p < 0.001) increased total thiol concentration and decreased the TNF-α and IL-1β concentrations, NO, and thiobarbituric acid reactive species. In the CFA-induced arthritis, FAEE 50 and 100 mg/kg significantly reduced the edema and the elevation paw time, a joint disability parameter, since second hour after arthritis induction (p < 0.001). FAEE presented rat joint protective activity in radiographic records (p < 0.001). The data suggest that the FAEE exerts anti-inflammatory activity by inhibiting leukocyte migration, oxidative stress reduction, and pro-inflammatory cytokines.

  17. Lipase immobilization on epoxy-activated poly(vinyl acetate-acrylamide) microspheres.

    PubMed

    Zhang, Dong-Hao; Peng, Li-Juan; Wang, Yun; Li, Ya-Qiong

    2015-05-01

    Poly(vinyl acetate-acrylamide) microspheres with an average diameter of 2-4μm were successfully prepared and characterized via SEM and FTIR. Then the microspheres were modified with epoxy groups through reacting with epichlorohydrin and used as carriers to covalently immobilize Candida rugosa lipase. The results revealed that agitation played an important role on epoxy activation and the immobilization ratio increased with the increase of the epoxy density. On the other hand, the specific activity of the immobilized lipase as well as the activity recovery declined gradually with the increase in the immobilization ratio from 72% to 93%, which were attributed to the steric hindrance effects caused by enzyme overloading. When epoxy density was 76μmol/g microsphere, the activity recovery reached the maximum at 47.5%, and the activity of the immobilized lipase was 261.3U/g microsphere. Moreover, the thermal stability of the immobilized lipase was much better than that of the free one, which indicated potential applications of the immobilized lipase.

  18. Effect of retinyl acetate on transglutaminase 2 activity in carcinogen treated rat liver.

    PubMed

    Aydin, O; Akyuz, F; Tekin, N; Ustuner, Mc; Degirmenci, I; Burukoglu, D; Ozden, H

    2016-07-01

    Transglutaminase 2 (TG2) has been implicated in wound healing, cellular differentiation, apoptosis and cell survival. TG2 activity increases following acute and chronic liver injury; however, the role of TG2 in tumors, is controversial. TG2 is a retinoid-inducible enzyme. We investigated the effects of retinyl acetate (RA) on the activity and levels of TG2 during the initiation and promotion stages of liver cancer. p-Dimethylaminoazobenzene (p-DAB) was used as initiator and 2, 3, 7, 8-tetrachlorodibenzo-p-dioxin (TCDD) was used as promoter in our model of carcinogenesis. Rats were divided into four groups of 24: control, corn oil control, p-DAB + TCDD, and p-DAB + TCDD + RA. Six rats from each group were sacrificed at days 30, 60, 90 and 120. TG2 activity decreased in the p-DAB + TCDD treated group, but TG2 immunostaining scores did not change by days 90 and 120. Neither TG2 enzyme activity nor the immunostaining score of TG2 protein changed in the tissues of the p-DAB + TCDD + RA group by days 90 and 120. TG2 activity was not be ameliorated by RA during the initiation or promotion stages of carcinogen induced liver cancer.

  19. Transition-state metal aryl bond stability determines regioselectivity in palladium acetate mediated C-H bond activation of heteroarenes.

    PubMed

    Petit, Alban; Flygare, Josh; Miller, Alex T; Winkel, Gerrit; Ess, Daniel H

    2012-07-20

    Density functional calculations reveal that the stability of developing metal aryl bonds in Pd(II)-acetate C-H activation transition states determines regioselectivity in arene and heteroarene compounds. This kinetic-thermodynamic connection explains the general preference for activation of the strongest C-H bond and provides the possibility for regioselectivity prediction.

  20. Batch Tests To Determine Activity Distribution and Kinetic Parameters for Acetate Utilization in Expanded-Bed Anaerobic Reactors

    PubMed Central

    Fox, Peter; Suidan, Makram T.

    1990-01-01

    Batch tests to measure maximum acetate utilization rates were used to determine the distribution of acetate utilizers in expanded-bed sand and expanded-bed granular activated carbon (GAC) reactors. The reactors were fed a mixture of acetate and 3-ethylphenol, and they contained the same predominant aceticlastic methanogen, Methanothrix sp. Batch tests were performed both on the entire reactor contents and with media removed from the reactors. Results indicated that activity was evenly distributed within the GAC reactors, whereas in the sand reactor a sludge blanket on top of the sand bed contained approximately 50% of the activity. The Monod half-velocity constant (Ks) for the acetate-utilizing methanogens in two expanded-bed GAC reactors was searched for by combining steady-state results with batch test data. All parameters necessary to develop a model with Monod kinetics were experimentally determined except for Ks. However, Ks was a function of the effluent 3-ethylphenol concentration, and batch test results demonstrated that maximum acetate utilization rates were not a function of the effluent 3-ethylphenol concentration. Addition of a competitive inhibition term into the Monod expression predicted the dependence of Ks on the effluent 3-ethylphenol concentration. A two-parameter search determined a Ks of 8.99 mg of acetate per liter and a Ki of 2.41 mg of 3-ethylphenol per liter. Model predictions were in agreement with experimental observations for all effluent 3-ethylphenol concentrations. Batch tests measured the activity for a specific substrate and determined the distribution of activity in the reactor. The use of steady-state data in conjunction with batch test results reduced the number of unknown kinetic parameters and thereby reduced the uncertainty in the results and the assumptions made. PMID:16348175

  1. Lipase Activity of Tropical Oilseed Plants for Ethyl Biodiesel Synthesis and Their Typo- and Regioselectivity.

    PubMed

    Nanssou Kouteu, Paul A; Baréa, Bruno; Barouh, Nathalie; Blin, Joël; Villeneuve, Pierre

    2016-11-23

    The aim of this work was to investigate lipase activities in crude extracts from Adansonia suarezensis, Adansonia grandidieri, Moringa drouhardii, Moringa oleifera, Jatropha mahafalensis, and Jatropha curcas seeds in ethanolysis and hydrolysis reactions. All crude extracts from germinated seeds showed both ethanolysis and hydrolysis activities. The influence of germination, the delipidation procedure, and the triacylglycerol/ethanol molar ratio on their ethanolysis activity was studied. Crude extracts of Jatropha and Adansonia seeds showed optimal activity at pH 8 with an optimum temperature of 30 and 40 °C, respectively. The study of the regioselectivity of crude extracts from J. mahafalensis and A. grandidieri seeds, which had the most active hydrolysis reaction, showed 1,3 regioselectivity in the hydrolysis reaction of vegetable oils. The crude extract from A. grandidieri seeds showed no typoselectivity, whereas the typoselectivity of the crude extract of J. mahafalensis seeds depended on the type of reaction.

  2. Grafting of poly[2-(tert-butylamino)ethyl methacrylate] onto polypropylene by reactive blending and antibacterial activity of the copolymer.

    PubMed

    Thomassin, Jean-Michel; Lenoir, Sandrine; Riga, Johan; Jérôme, Robert; Detrembleur, Christophe

    2007-04-01

    To combine low cost, good mechanical properties, and antibacterial activity in one material, a nonquaternized polymeric biocide, i.e., poly[2-(tert-butylamino)ethyl methacrylate] (PTBAEMA), was dispersed within a commodity plastic, i.e., polypropylene (PP). The high immiscibility of the two polymers was tackled by reactive compatibilization and thus by reaction of commercially available maleic anhydride grafted polypropylene with primary amine-end-capped PTBAEMA. This reactive polymethacrylate was synthesized by atom-transfer radical polymerization with an azide-containing initiator. The azide end group was converted into a primary amine by the Huisgen [3 + 2] cycloaddition of propargylamine. The accordingly formed PP-g-PTBAEMA copolymer was melt dispersed within neat PP and processed as fibers, whose antimicrobial properties were assessed by the viable cell counting method against Escherichia coli. The antibacterial activity was long-lasting as a result of the anchoring of the PTBAEMA chains onto PP, which prevented them from being released from the surface of the fibers.

  3. Effect of acetic acid present in bagasse hydrolysate on the activities of xylose reductase and xylitol dehydrogenase in Candida guilliermondii.

    PubMed

    Lima, Luanne Helena Augusto; das Graças de Almeida Felipe, Maria; Vitolo, Michele; Torres, Fernando Araripe Gonçalves

    2004-11-01

    The first two steps in xylose metabolism are catalyzed by NAD(P)H-dependent xylose reductase (XR) (EC 1.1.1.21) and NAD(P)-dependent xylitol dehydrogenase (XDH) (EC 1.1.1.9), which lead to xylose-->xylitol-->xylulose conversion. Xylitol has high commercial value, due to its sweetening and anticariogenic properties, as well as several clinical applications. The acid hydrolysis of sugarcane bagasse allows the separation of a xylose-rich hemicellulosic fraction that can be used as a substrate for Candida guilliermondii to produce xylitol. However, the hydrolysate contains acetic acid, an inhibitor of microbial metabolism. In this study, the effect of acetic acid on the activities of XR and XDH and on xylitol formation by C. guilliermondii were studied. For this purpose, fermentations were carried out in bagasse hydrolysate and in synthetic medium. The activities of XR and XDH were higher in the medium containing acetic acid than in control medium. Moreover, none of the fermentative parameters were significantly altered during cell culture. It was concluded that acetic acid does not interfere with xylitol formation since the increase in XR activity is proportional to XDH activity, leading to a greater production of xylitol and its subsequent conversion to xylulose.

  4. Rapid isolation of a facultative anaerobic electrochemically active bacterium capable of oxidizing acetate for electrogenesis and azo dyes reduction.

    PubMed

    Shen, Nan; Yuan, Shi-Jie; Wu, Chao; Cheng, Yuan-Yuan; Song, Xiang-Ning; Li, Wen-Wei; Tong, Zhong-Hua; Yu, Han-Qing

    2014-05-01

    In this study, 27 strains of electrochemically active bacteria (EAB) were rapidly isolated and their capabilities of extracellular electron transfer were identified using a photometric method based on WO3 nanoclusters. These strains caused color change of WO3 from white to blue in a 24-well agar plate within 40 h. Most of the isolated EAB strains belonged to the genera of Aeromonas and Shewanella. One isolate, Pantoea agglomerans S5-44, was identified as an EAB that can utilize acetate as the carbon source to produce electricity and reduce azo dyes under anaerobic conditions. The results confirmed the capability of P. agglomerans S5-44 for extracellular electron transfer. The isolation of this acetate-utilizing, facultative EBA reveals the metabolic diversity of environmental bacteria. Such strains have great potential for environmental applications, especially at interfaces of aerobic and anaerobic environments, where acetate is the main available carbon source.

  5. Electrochemical performance of microporous and mesoporous activated carbons in neat and diluted 1-ethyl-3-methylimidazolium tetrafluoroborate

    NASA Astrophysics Data System (ADS)

    Kumagai, Seiji; Hatomi, Masaki; Tashima, Daisuke

    2017-03-01

    1-Ethyl-3-methylimidazolium tetrafluoroborate (EMIm·BF4), neat and diluted with propylene carbonate to 1 mol L-1, have been employed as electrolytes of electrical double-layer capacitors (EDLCs). The effects of microporosity and mesoporosity in activated carbon (AC) electrodes on the capacitive and resistive performances upon the use of neat and diluted EMIm·BF4 have been explored. In addition to cyclic voltammetry and galvanostatic charge-discharge tests, electrochemical impedance spectroscopy has been performed employing Kang's equivalent circuit model consisting of three resistances, three constant phase elements, and one bounded Warburg impedance. The overall impedance of the EDLC cell was separated into components of intrinsic resistance, bulk electrolyte, diffusion layer, and Helmholtz layer. The specific capacitance and the equivalent series resistance (ESR) of mesoporous AC were found to be highly dependent on the rate of ionic transfer. Lower cell voltage was identified as being responsible for lower specific capacitance and larger ESR of mesoporous AC, which was similarly seen in the neat and diluted EMIm·BF4, and could be alleviated by increasing the cell voltage. The inferior rate performance and the cell-voltage-dependent performance of mesoporous AC, which were more distinctly observed in the neat EMIm·BF4, could be attributed to the lower mobility of EMIm+ and BF4- in mesopores.

  6. Activity coefficients at infinite dilution of organic solutes in the ionic liquid 1-ethyl-3-methyl-imidazolium nitrate.

    PubMed

    Sobota, Marek; Dohnal, Vladimír; Vrbka, Pavel

    2009-04-02

    Infinite dilution activity coefficients gamma(1)(infinity) and gas-liquid partition coefficients K(L) of 30 selected hydrocarbons, alcohols, ketones, ethers, esters, haloalkanes, nitrogen- and sulfur-containing compounds in the ionic liquid (IL) 1-ethyl-3-methylimidazolium nitrate [EMIM][NO(3)] were determined by gas-liquid chromatography at five temperatures in the range from 318.15 to 353.15 K. Relative contribution of adsorption at gas-liquid interphase to the overall solute retention, as examined by varying sample size and IL loading in the column, was found negligible. Partial molar excess enthalpies and entropies at infinite dilution were derived from the temperature dependence of the gamma(1)(infinity) values. The linear free energy relationship (LFER) solvation model was used to correlate successfully the KL values. The LFER correlation parameters and excess thermodynamic functions were analyzed to disclose molecular interactions operating between the IL and the individual solutes. In addition, the promising potential of [EMIM][NO(3)] for applications in solvent-aided separation processes was identified, the selectivities of [EMIM][NO(3)] for separation of aromatic hydrocarbons and thiophene from saturated hydrocarbons ranking among the highest ever observed with ILs or molecular solvents.

  7. In vitro and in vivo trypanocidal activity of the ethyl esters of N-allyl and N-propyl oxamates using different Trypanosoma cruzi strains.

    PubMed

    Aguirre-Alvarado, Charmina; Zaragoza-Martínez, Fabiola; Rodríguez-Páez, Lorena; Nogueda, Benjamín; Baeza, Isabel; Wong, Carlos

    2007-04-01

    The trypanocidal activity of N-allyl (NAOx) and N-propyl (NPOx) oxamates and that of the ethyl esters ofN-allyl (Et-NAOx) and N-propyl (Et-NPOx) oxamates were tested on cultured epimastigotes (in vitro) and murine trypanosomiasis (in vivo) using five different T. cruzi strains. NAOx and NPOx did not penetrate intact epimastigotes and therefore we were not able to detect any trypanocidal effect with these oxamates. Whereas the ethyl esters (Et-NAOx and Et-NPOx), acting as prodrugs, exhibited in vitro and in vivo trypanocidal activity on the five tested T. cruzi strains. On the contrary, when Nifurtimox and Benznidazole used as reference drugs were tested, we found that only three of the five tested T cruzi strains were affected, whereas the other two strains, Miguz and Compostela, were resistant to the in vitro and in vivo trypanocidal activity of these compounds.

  8. [Research of imidazo[1,2-a]benzimidazole derivatives. XXX. Synthesis and properties of (imidazo[1,2-a]benzimidazolyl-2)acetic acid derivatives].

    PubMed

    Anisimova, V A; Tolpygin, I E; Spasov, A A; Serdiuk, T S; Sukhov, A G

    2011-01-01

    Ethyl esters of (9-subtituted-imidazo[1,2-a]benzimidazolyl-2)acetic acids were synthesized. The chemical properties of these esters (hydrolysis, decarboxylation, hydrazinolysis) and biological activity (fungicidal, antimicrobial, antiarrhythmic activity, and also affects on the brain rhythmogenesis) of the prepared compounds were studied.

  9. Nadroparin sodium activates Nrf2/HO-1 pathway in acetic acid-induced colitis in rats.

    PubMed

    Yalniz, Mehmet; Demirel, Ulvi; Orhan, Cemal; Bahcecioglu, Ibrahim Halil; Ozercan, Ibrahim Hanefi; Aygun, Cem; Tuzcu, Mehmet; Sahin, Kazim

    2012-06-01

    Effects of nadroparin sodium, a low molecular weight heparin, in colitis was investigated by analyzing proteins implicated in nuclear factor E2-related factor-2/heme oxygenase-1 (Nrf2/HO-1) and nuclear factor kappa B (NF-κB) pathways. Twenty-eight rats were used. Colitis was induced by acetic acid (AA). Nadroparin sodium was given to prevention and treatment groups in addition to AA. Colitis was assessed histologically and levels of proteins were analyzed with Western blot. Nadroparin not only prevented and ameliorated the AA-induced colitis histopathologically but also decreased expression of colon NF-κB, activator protein-1, cyclooxygenase-2, tumor necrosis factor-alpha, and IL-6, which were significantly increased in group AA compared to control. The accumulation of Nrf2 in nuclear fraction and HO-1 found low in group AA was increased with nadroparin (p < 0.05). The mean malondialdehyde level increased with AA and was decreased significantly with nadroparin prevention and treatment (p < 0.001). Nadroparin sodium has both protective and therapeutic effects against colonic inflammation via exerting anti-oxidative and anti-inflammatory effects by modulating Nrf2/HO-1 and NF-κB pathways.

  10. Effects of Indole-3-Acetic Acid on the Transcriptional Activities and Stress Tolerance of Bradyrhizobium japonicum

    PubMed Central

    Donati, Andrew J.; Lee, Hae-In; Leveau, Johan H. J.; Chang, Woo-Suk

    2013-01-01

    A genome-wide transcriptional profile of Bradyrhizobium japonicum, the nitrogen-fixing endosymbiont of the soybean plant, revealed differential expression of approximately 15% of the genome after a 1 mM treatment with the phytohormone indole-3-acetic acid (IAA). A total of 1,323 genes were differentially expressed (619 up-regulated and 704 down-regulated) at a two-fold cut off with q value ≤ 0.05. General stress response genes were induced, such as those involved in response to heat, cold, oxidative, osmotic, and desiccation stresses and in exopolysaccharide (EPS) biosynthesis. This suggests that IAA is effective in activating a generalized stress response in B. japonicum. The transcriptional data were corroborated by the finding that stress tolerance of B. japonicum in cell viability assays was enhanced when pre-treated with 1 mM IAA compared to controls. The IAA treatment also stimulated biofilm formation and EPS production by B. japonicum, especially acidic sugar components in the total EPS. The IAA pre-treatment did not influence the nodulation ability of B. japonicum. The data provide a comprehensive overview of the potential transcriptional responses of the symbiotic bacterium when exposed to the ubiquitous hormone of its plant host. PMID:24098533

  11. Glatiramer acetate inhibits degradation of collagen II by suppressing the activity of interferon regulatory factor-1.

    PubMed

    Lu, Huading; Zeng, Chun; Zhao, Huiqing; Lian, Liyi; Dai, Yuhu

    2014-06-06

    Pro-inflammatory cytokines such as tumor necrosis factor-alpha (TNF-α) is considered to be the major one contributing to the process of development of osteoarthritis (OA).Interferon regulatory factor 1 (IRF-1) is an important transcriptional factor accounting for inflammation response induced by TNF-α. The physiological function of IRF-1 in OA is still unknown. In this study, we reported that the expression levels of IRF-1 in OA chondrocytes were significantly higher compared to those in normal chondrocytes, which was reversed by treatment with Glatiramer acetate (GA), a licensed clinical drug for treating patients suffering from multiple sclerosis (MS). We also found that GA is able to attenuate the upregulation of IRF-1 induced by TNF-α. Matrix metalloproteinase13 (MMP-13) is one of the downstream target genes of IRF-1, which can induce the degradation of collagen II. Importantly, our results indicated that GA suppressed the expression of MMP-13 as well as the degradation of collagen II. In addition, GA also suppressed TNF-α-induced production of NO and expression of iNOS. Finally, we found that the inhibition of STAT1 activation played a critical role in the inhibitory effects of GA on the induction of IRF-1 and MMP-13. These data suggest that GA might have a potential effect in therapeutic OA.

  12. Cytotoxicity and antitumour activity of 5-fluorouracil-loaded polyhydroxybutyrate and cellulose acetate phthalate blend microspheres.

    PubMed

    Chaturvedi, Kiran; Tripathi, Santosh Kumar; Kulkarni, Anandrao R; Aminabhavi, Tejraj M

    2013-01-01

    Pharmacokinetics, biodistribution and antitumour activity of 5-fluorouracil (5-FU)-loaded polyhydroxybutyrate (PHB) and cellulose acetate phthalate (CAP) blend microspheres were investigated in chemically induced colorectal cancer in albino male Wistar rats and compared with pristine 5-FU given as a suspension. The microspheres were characterised for particle size, encapsulation efficiency, in vitro release and in vitro cytotoxicity on human HT-29 colon cancer cell line. Spherical particles with a mean size of 44 ± 11 µm were obtained that showed sustained release of 5-FU. A high concentration of 5-FU was achieved in colonic tissues and significant reduction in tumour volume and multiplicity were observed in animals treated with 5-FU-loaded microspheres. The decreased levels of plasma albumin, creatinine, leucocytopenia and thrombocytopenia were observed in animals for 5-FU microspheres compared to the standard 5-FU formulation. The results suggest the extended release of 5-FU from the PHB-CAP blend microspheres in colonic region to enhance the antitumour efficacy.

  13. Effects of indole-3-acetic acid on the transcriptional activities and stress tolerance of Bradyrhizobium japonicum.

    PubMed

    Donati, Andrew J; Lee, Hae-In; Leveau, Johan H J; Chang, Woo-Suk

    2013-01-01

    A genome-wide transcriptional profile of Bradyrhizobium japonicum, the nitrogen-fixing endosymbiont of the soybean plant, revealed differential expression of approximately 15% of the genome after a 1 mM treatment with the phytohormone indole-3-acetic acid (IAA). A total of 1,323 genes were differentially expressed (619 up-regulated and 704 down-regulated) at a two-fold cut off with q value ≤ 0.05. General stress response genes were induced, such as those involved in response to heat, cold, oxidative, osmotic, and desiccation stresses and in exopolysaccharide (EPS) biosynthesis. This suggests that IAA is effective in activating a generalized stress response in B. japonicum. The transcriptional data were corroborated by the finding that stress tolerance of B. japonicum in cell viability assays was enhanced when pre-treated with 1 mM IAA compared to controls. The IAA treatment also stimulated biofilm formation and EPS production by B. japonicum, especially acidic sugar components in the total EPS. The IAA pre-treatment did not influence the nodulation ability of B. japonicum. The data provide a comprehensive overview of the potential transcriptional responses of the symbiotic bacterium when exposed to the ubiquitous hormone of its plant host.

  14. Electrospun curcumin-loaded cellulose acetate/polyvinylpyrrolidone fibrous materials with complex architecture and antibacterial activity.

    PubMed

    Tsekova, Petya B; Spasova, Mariya G; Manolova, Nevena E; Markova, Nadya D; Rashkov, Iliya B

    2017-04-01

    Novel fibrous materials from cellulose acetate (CA) and polyvinylpyrrolidone (PVP) containing curcumin (Curc) with original design were prepared by one-pot electrospinning or dual spinneret electrospinning. The electrospun materials were characterized by scanning electron microscopy (SEM), fluorescence microscopy, Fourier transform infrared spectroscopy (FTIR), ultraviolet-visible spectroscopy (UV-Vis), differential scanning calorimetry (DSC), water contact angle measurements, and microbiological tests. It was found that the incorporation of Curc into the CA and PVP solutions resulted in an increase of the solution viscosity and obtaining fibers with larger diameters (ca. 1.5μm) compared to the neat CA (ca. 800nm) and PVP fibers (ca. 500nm). The incorporation of PVP resulted in increased hydrophilicity of the fibers and in faster Curc release. Curc was found in the amorphous state in the Curc-containing fibers and these mats exhibited antibacterial activity against Staphylococcus aureus (S. aureus). The results suggest that, due to their complex architecture, the obtained new antibacterial materials are suitable for wound dressing applications, which necessitate diverse release behaviors of the bioactive compound.

  15. Arsenic (III) adsorption on iron acetate coated activated alumina: thermodynamic, kinetics and equilibrium approach

    PubMed Central

    2013-01-01

    The adsorption potential of iron acetate coated activated alumina (IACAA) for removal of arsenic [As (III)] as arsenite by batch sorption technique is described. IACAA was characterized by XRD, FTIR, EDAX and SEM instruments. Percentage adsorption on IACAA was determined as a function of pH, contact time and adsorbent dose. The study revealed that the removal of As (III) was best achieved at pH =7.4. The initial As (III) concentration (0.45 mg/L) came down to less than 0.01 mg/L at contact time 90 min with adsorbent dose of 1 g/100 mL. The sorption was reasonably explained with Langmuir and Freundlich isotherms. The thermodynamic parameters such as ΔG 0 , ΔH 0 , ΔS 0 and E a were calculated in order to understand the nature of sorption process. The sorption process was found to be controlled by pseudo-second order and intraparticle diffusion models. PMID:24359995

  16. Heat-activated persulfate oxidation of methyl- and ethyl-parabens: Effect, kinetics, and mechanism.

    PubMed

    Chen, Yiqun; Deng, Pinya; Xie, Pengchao; Shang, Ran; Wang, Zongping; Wang, Songlin

    2017-02-01

    We evaluated the degradation of methylparaben (MeP) and ethylparaben (EtP), two representative parabens, using the heat-activated persulfate system in a laboratory. Both sulfate and hydroxyl radicals contributed to the removal of the two parabens. The degradations of both MeP and EtP were improved by increasing the heating temperature or persulfate dose in accordance with a pseudo-first-order reaction model. The oxidation efficiency of parabens was found to be pH-dependent; decreasing in the order pH 5.0 > 7.0 > 9.0. The presence of chloride, bicarbonate, or humic acid was found to inhibit the degradation of the two parabens to some extent because of competition for the reactive radicals, with humic acid having the most serious effect. Dealkylation of the methyl unit, decarboxylation of the carboxylic group, and subsequent hydrolysis are proposed to be involved in the degradation pathway of MeP. The results suggest that the heat-activated persulfate system might be efficiently applied in the treatment of paraben-containing water samples. This was also supported by the results of applying this system to treat a real water sample containing both MeP and EtP.

  17. Antimicrobial Activity of Few Medicinal Plants against Clinically Isolated Human Cariogenic Pathogens—An In Vitro Study

    PubMed Central

    Jebashree, H. Shyla; Kingsley, S. Jayasurya; Sathish, Emmanuel S.; Devapriya, D.

    2011-01-01

    Hexane, ethyl acetate, ethanol and methanol extracts of Psidium guajava, Terminalia chebula, Mimusops elengi and Achyranthes aspera were tested against the dental caries causing bacteria Streptococcus mutans and fungus Candida albicans isolated from caries infected patients. All the four extracts of P. guajava showed activity against both S. mutans and C. albicans. Maximum zone of inhibition was observed in ethyl acetate of P. guajava. The four extracts of T. chebula and M. elengi showed antibacterial activity against S. mutans. M. elengi extracts and ethanol extract of T. chebula did not show any antifungal activity against C. albicans. Except for the hexane extract of A. aspera, the other three extracts showed activity against the tested microbes. The ethyl acetate P. guajava leaf extract showed the minimum inhibitory concentration (MIC) against S. mutans to be <0.076 mg/mL in both MHB and BHI. The P. guajava ethyl acetate extract was subjected to GC-MS. PMID:21991479

  18. Flecainide acetate acetic acid solvates.

    PubMed

    Veldre, Kaspars; Actiņs, Andris; Eglite, Zane

    2011-02-01

    Flecainide acetate forms acetic acid solvates with 0.5 and 2 acetic acid molecules. Powder X-ray diffraction, differential thermal analysis/thermogravimetric, infrared, and potentiometric titration were used to determine the composition of solvates. Flecainide acetate hemisolvate with acetic acid decomposes to form a new crystalline form of flecainide acetate. This form is less stable than the already known polymorphic form at all temperatures, and it is formed due to kinetic reasons. Both flecainide acetate nonsolvated and flecainide acetate hemisolvate forms crystallize in monoclinic crystals, but flecainide triacetate forms triclinic crystals. Solvate formation was not observed when flecainide base was treated with formic acid, propanoic acid, and butanoic acid. Only nonsolvated flecainide salts were obtained in these experiments.

  19. Investigation of the pore structure and morphology of cellulose acetate membranes using small-angle neutron scattering. 1: Cellulose acetate active layer membranes

    SciTech Connect

    Kulkarni, S.; Krause, S. ); Wignall, G.D. . Solid State Div.); Hammouda, B. . Center for High Resolution Neutron Scattering)

    1994-11-07

    The structure of ultrathin cellulose acetate membranes, known as active layer membranes, has been investigated using small-angle neutron scattering. These membranes are known to have structural and functional similarity to the surface or skin layer in commercial reverse-osmosis (RO) membranes and hence are useful model systems for understanding the structure of the RO membrane skin layer. Active layer membranes were studied after swelling them with either D[sub 2]O or CD[sub 3]OD. The results in both cases clearly indicated the presence of very small (10--20 [angstrom]) porous structures in the membrane. The presence of such pores has been a subject of long-standing controversy in this area. The data were analyzed using a modified Debye-Bueche analysis and the resultant membrane structure was seen to agree well with structural information from electron microscopic studies. Finally, a possible explanation for the differences in scattering observed between the D[sub 2]O swollen membranes and the CD[sub 3]OD swollen membranes has been presented.

  20. Effect of anthropogenic activity on formate and acetate levels in precipitation at four sites in Agra, India

    NASA Astrophysics Data System (ADS)

    Kumar, Nandini; Kulshreshta, U. C.; Saxena, A.; Kumari, K. M.; Srivastava, S. S.

    Twenty-four-hour precipitation samples from four sites: Dayalbagh (DB), Hari Parvat (HP), Taj Mahal (TM) and Udyog Kendra (UK) in Agra city, during the monsoon season (July-September) of 1991, were analysed for formate and acetate. Each site was representative of a different level of anthropogenic activity. The formate/acetate ratio observed appeared to be characteristic of the dominant activity at the site; the geometric means of the formate/acetate ratios calculated for individual samples were 0.99, 0.17, 0.83 and 0.21 for DB, HP, TM and UK, respectively. These corresponded to the level of pollution at the site. Direct acetate inputs from extensive combustion and automobile exhaust could contribute to elevated levels of the species at two of the four sites. Another possible indirect input could be from the alkaline hydrolysis of PAN, aided by relatively high pH values of rain water (volume-weighted averages = 6.79, 6.69, 7.22, 7.15) at the four sites.

  1. Effect of malonate and p-chlorophenoxy acetic acid on hepatic succinic dehydrogenase activity of ageing lizards.

    PubMed

    Jena, B S; Patnaik, B K

    1990-01-01

    The degree of inhibition of hepatic succinic dehydrogenase activity by malonate, a competitive inhibitor, did not differ between young and middle-aged lizards. On the other hand, the same parameter increased significantly between middle-aged and old lizards. The percent inhibition of enzyme activity by p-chlorophenoxy acetic acid was also age-dependent, being higher in middle-aged and old than in young lizards.

  2. Biological activities of Solanum pseudocapsicum (Solanaceae) against cotton bollworm, Helicoverpa armigera Hübner and armyworm, Spodoptera litura Fabricius (Lepidotera: Noctuidae)

    PubMed Central

    Jeyasankar, Alagarmalai; Premalatha, Selvaraj; Elumalai, Kuppusamy

    2012-01-01

    Objective To evaluate the antifeedant, insecticidal and growth inhibition activities of Solanum pseudocapsicum (S. pseudocapsicum) seed extracts against Spodoptera litura (S. litura) and Helicoverpa armigera (H. armigera). Methods Hexane, diethyl ether, dichloromethane and ethyl acetate seed extracts were prepared and tested for antifeedant, insecticidal and growth inhibitory activities against fourth instar larvae of S. litura and H. armigera. Results Ethyl acetate extract showed promising antifeedant and insecticidal activities against S. litura and H. armigera. Percentage of deformed larvae, pupae and adults were maximum in treatment of ethyl acetate extract. Percentage of successful adult emergence was deteriorated by seeds on extract treated larvae. Conclusions Ethyl acetate extracts of S. pseudocapsicum, showed higher efficiency of antifeedant, insecticidal and growth inhibition activities. Hence, it can be used to controll agricultural insect pests, S. litura and H. armigera. PMID:23593579

  3. Zulu medicinal plants with antibacterial activity.

    PubMed

    Kelmanson, J E; Jäger, A K; van Staden, J

    2000-03-01

    Aqueous, methanolic and ethyl acetate extracts of 14 plants used in traditional Zulu medicine for treatment of ailments of an infectious nature were screened for antibacterial activity. Most of the activity detected was against gram-positive bacteria. Tuber bark extracts of Dioscorea sylvatica had activity against gram-negative Escherichia coli and extracts of Dioscorea dregeana, Cheilanthes viridis and Vernonia colorata were active against Pseudomonas aeruginosa. The highest antibacterial activity was found in extracts of C. viridis, D. dregeana, D. silvatica, Melianthus comosus and V. colorata. In general, methanolic extracts exhibited higher activity than aqueous and ethyl acetate extracts.

  4. Polycyclic Aromatic Hydrocarbon Affects Acetic Acid Production during Anaerobic Fermentation of Waste Activated Sludge by Altering Activity and Viability of Acetogen.

    PubMed

    Luo, Jingyang; Chen, Yinguang; Feng, Leiyu

    2016-07-05

    Till now, almost all the studies on anaerobic fermentation of waste activated sludge (WAS) for bioproducts generation focused on the influences of operating conditions, pretreatment methods and sludge characteristics, and few considered those of widespread persistent organic pollutants (POPs) in sludge, for example, polycyclic aromatic hydrocarbons (PAHs). Herein, phenanthrene, which was a typical PAH and widespread in WAS, was selected as a model compound to investigate its effect on WAS anaerobic fermentation for short-chain fatty acids (SCFAs) accumulation. Experimental results showed that the concentration of SCFAs derived from WAS was increased in the presence of phenanthrene during anaerobic fermentation. The yield of acetic acid which was the predominant SCFA in the fermentation reactor with the concentration of 100 mg/kg dry sludge was 1.8 fold of that in the control. Mechanism exploration revealed that the present phenanthrene mainly affected the acidification process of anaerobic fermentation and caused the shift of the microbial community to benefit the accumulation of acetic acid. Further investigation showed that both the activities of key enzymes (phosphotransacetylase and acetate kinase) involved in acetic acid production and the quantities of their corresponding encoding genes were enhanced in the presence of phenanthrene. Viability tests by determining the adenosine 5'-triphosphate content and membrane potential confirmed that the acetogens were more viable in anaerobic fermentation systems with phenanthrene, which resulted in the increased production of acetic acid.

  5. Dispersibility and emulsion-stabilizing effect of cellulose nanowhiskers esterified by vinyl acetate and vinyl cinnamate.

    PubMed

    Sèbe, Gilles; Ham-Pichavant, Frédérique; Pecastaings, Gilles

    2013-08-12

    The surface of cotton cellulose nanowhiskers (CNW's) was esterified by vinyl acetate (VAc) and vinyl cinnamate (VCin), in the presence of potassium carbonate as catalyst. Reactions were performed under microwave activation and monitored by Fourier transform infrared (FT-IR) spectroscopy. The supramolecular structure of CNW's before and after modification was characterized by X-ray diffraction (XRD) and atomic force microscopy (AFM). Distinctively from the acetylation treatment, an increase in particles dimensions was noted after esterification with VCin, which was assigned to π-π stacking interactions that may exist between cinnamoyl moieties. The dispersibility and emulsion stabilizing effect of acylated CNW's was examined in ethyl acetate, toluene, and cyclohexane, three organic solvents of medium to low polarity. The acylated nanoparticles could never be dispersed in toluene nor cyclohexane, but they formed stable dispersions in ethyl acetate while remaining dispersible in water. Stable ethyl acetate-in-water, toluene-in-water, and cyclohexane-in-water emulsions were successfully prepared with CNW's grafted with acetyl moieties, whereas the VCin-treated particles could stabilize only the cyclohexane-in-water emulsions. The impact of esterification treatment on emulsion stability and droplets size was particularly discussed.

  6. Methanosarcinaceae and Acetate-Oxidizing Pathways Dominate in High-Rate Thermophilic Anaerobic Digestion of Waste-Activated Sludge

    PubMed Central

    Ho, Dang P.; Jensen, Paul D.

    2013-01-01

    This study investigated the process of high-rate, high-temperature methanogenesis to enable very-high-volume loading during anaerobic digestion of waste-activated sludge. Reducing the hydraulic retention time (HRT) from 15 to 20 days in mesophilic digestion down to 3 days was achievable at a thermophilic temperature (55°C) with stable digester performance and methanogenic activity. A volatile solids (VS) destruction efficiency of 33 to 35% was achieved on waste-activated sludge, comparable to that obtained via mesophilic processes with low organic acid levels (<200 mg/liter chemical oxygen demand [COD]). Methane yield (VS basis) was 150 to 180 liters of CH4/kg of VSadded. According to 16S rRNA pyrotag sequencing and fluorescence in situ hybridization (FISH), the methanogenic community was dominated by members of the Methanosarcinaceae, which have a high level of metabolic capability, including acetoclastic and hydrogenotrophic methanogenesis. Loss of function at an HRT of 2 days was accompanied by a loss of the methanogens, according to pyrotag sequencing. The two acetate conversion pathways, namely, acetoclastic methanogenesis and syntrophic acetate oxidation, were quantified by stable carbon isotope ratio mass spectrometry. The results showed that the majority of methane was generated by nonacetoclastic pathways, both in the reactors and in off-line batch tests, confirming that syntrophic acetate oxidation is a key pathway at elevated temperatures. The proportion of methane due to acetate cleavage increased later in the batch, and it is likely that stable oxidation in the continuous reactor was maintained by application of the consistently low retention time. PMID:23956388

  7. Acaricidal activity of Palicourea marcgravii, a species from the Amazon forest, on cattle tick Rhipicephalus (Boophilus) microplus.

    PubMed

    Silva, Wilson Castro; Martins, João Ricardo de Souza; Cesio, Maria Veronica; Azevedo, João Lúcio; Heinzen, Horacio; de Barros, Neiva Monteiro

    2011-06-30

    Leaves of Palicourea marcgravii were extracted successively with hexane, ethyl acetate and ethanol in order to evaluate their acaricidal activity on larvae and adult stages of the cattle tick Rhipicephalus (Boophilus) microplus. The ethyl acetate extract showed the highest bioactivity of the tested extracts, which contained 0.12% monofluoroacetic acid. On engorged female, the ethyl acetate extract showed a lethal concentration 50% - LC(50)=30.08 mg ml(-1), inhibitory concentration 50% - IC(50)=5.79 mg ml(-1) and lethal time 50% - LT(50)=4.72 days; 100% reproduction was controlled at concentrations of 50 mg ml(-1) and on larvae the ethyl acetate extract showed a LC(50)=2.46 mg ml(-1). No alkaloids were detected in any of the extracts. This is the first report on the acaricidal activity of P. marcgravii extracts against R. microplus as well as the acaricidal properties of a plant species containing monofluoroacetic acid.

  8. Active Oxygen Metabolites and Thromboxane in Phorbol Myristate Acetate Toxicity to the Isolated, Perfused Rat Lung.

    NASA Astrophysics Data System (ADS)

    Carpenter, Laurie Jean

    When administered intravenously or intratracheally to rats, rabbits and sheep, phorbol myristate acetate (PMA) produces changes in lung morphology and function are similar to those seen in humans with the adult respiratory distress syndrome (ARDS). Therefore, it is thought that information about the mechanism of ARDS development can be gained from experiments using PMA-treated animals. Currently, the mechanisms by which PMA causes pneumotoxicity are unknown. Results from other studies in rabbits and in isolated, perfused rabbit lungs suggest that PMA-induced lung injury is mediated by active oxygen species from neutrophils (PMN), whereas studies in sheep and rats suggest that PMN are not required for the toxic response. The role of PMN, active oxygen metabolites and thromboxane (TxA_2) in PMA-induced injury to isolated, perfused rat lungs (IPLs) was examined in this thesis. To determine whether PMN were required for PMA to produce toxicity to the IPL, lungs were perfused for 30 min with buffer containing various concentrations of PMA (in the presence or absence of PMN). When concentrations >=q57 ng/ml were added to medium devoid of added PMN, perfusion pressure and lung weight increased. When a concentration of PMA (14-28 ng/ml) that did not by itself cause lungs to accumulate fluid was added to the perfusion medium containing PMN (1 x 10 ^8), perfusion pressure increased, and lungs accumulated fluid. These results indicate that high concentrations of PMA produce lung injury which is independent of PMN, whereas injury induced by lower concentrations is PMN-dependent. To examine whether active oxygen species were involved in mediating lung injury induced by PMA and PMN, lungs were coperfused with the oxygen radical scavengers SOD and/or catalase. Coperfusion with either or both of these enzymes totally protected lungs against injury caused by PMN and PMA. These results suggest that active oxygen species (the hydroxyl radical in particular), mediate lung injury in

  9. Mesoxalaldehyde acetals

    SciTech Connect

    Gordeeva, G.N.; Kalashnikov, S.M.; Popov, Yu.N.; Kruglov, E.A.; Imashev, U.B.

    1987-11-10

    The treatment of methylglyoxal acetals by alkyl nitrites in the presence of the corresponding aliphatic alcohols and hydrochloric acid leads to the formation of linear mesoxalaldehyde acetals, whose structure was established by NMR spectroscopy and mass spectrometry. The major pathways for the decomposition of these molecules upon electron impact were established.

  10. Antimicrobial activity of the solvent fractions from Bulbine natalensis Tuber.

    PubMed

    Yakubu, M T; Mostafa, M; Ashafa, A O T; Afolayan, A J

    2012-01-01

    Bulbine natalensis Baker has been acclaimed to be used as an antimicrobial agent in the folklore medicine of South Africa without scientific evidence to substantiate or refute this claim. In view of this, the in vitro antimicrobial activity of solvent fractions (ethanol, ethyl acetate, n-butanol and water) from Bulbine natalensis Tuber against 4 Gram positive and 12 Gram negative bacteria as well as 3 fungal species were investigated using agar dilution. The ethanolic extract, n-butanol and ethyl acetate fractions inhibited 75, 87.5 and 100% respectively of the bacterial species in this study. The ethanolic, n-butanol and ethyl acetate fractions produced growth inhibition at MIC range of 1-10, 3-10 as well as 1 and 5 mg/ml respectively whereas the water fraction did not inhibit the growth of any of the bacterial species. Again, it was only the ethyl acetate fraction that inhibited the growth of Shigelli flexneri, Staphyloccus aureus and Escherichia coli. The ethanolic, ethyl acetate and n-butanolic fractions dose dependently inhibited the growth of Aspergillus niger and A. flavus whereas the water fraction produced 100% growth inhibition of the Aspergillus species at all the doses investigated. In contrast, no growth inhibition was produced on Candida albicans. The growth inhibition produced by the solvent fractions of B. natalensis Tuber in this study thus justifies the acclaimed use of the plant as an antimicrobial agent. The ethyl acetate fraction was the most potent.

  11. Multiple hormonal activities of UV filters and comparison of in vivo and in vitro estrogenic activity of ethyl-4-aminobenzoate in fish.

    PubMed

    Kunz, Petra Y; Fent, Karl

    2006-10-12

    UV filters have been detected in surface water, wastewater and fish, and some of them are estrogenic in fish. At present, little is known about their additional hormonal activities in different hormonal receptor systems despite their increasing use and environmental persistence. Besides estrogenic activity, UV filters may have additional activities, both agonistic and antagonistic in aquatic organisms. In our study, we investigate a series of UV filters for multiple hormonal activities in vitro in human receptor systems and evaluate the predictive value of these findings for the activity in fish in vitro and in vivo. First we systematically analysed the estrogenic, antiestrogenic, androgenic, and antiandrogenic activity of 18 UV filters and one metabolite in vitro at non-cytotoxic concentrations with recombinant yeast systems carrying either a human estrogen (hERalpha) or androgen receptor (hAR). All 19 compounds elicited hormonal activities, surprisingly most of them multiple activities. We found 10 UV-filters having agonistic effects towards the hERalpha. Surprisingly, we identified for the first time six UV filters with androgenic activities and many of them having pronounced antiestrogenic and antiandrogenic activities. As much as 17 compounds inhibited 4,5-dihydrotestosterone activity in the hAR assay, while 14 compounds inhibited estradiol activity in the hERalpha assay, indicating antiandrogenic and antiestrogenic activity, respectively. In particular, the antiandrogenic activities of phenyl- and benzyl salicylate, benzophenone-1 and -2, and of 4-hydroxybenzophenone were higher than that of flutamide, a known hAR antagonist. In a second series of experiments, we investigated the predictive power of the hERalpha assay for aquatic organisms by further investigating the estrogenic UV filter ethyl 4-aminobenzoate (Et-PABA) in vitro and in vivo in fish. Et-PABA showed estrogenic activity in a recombinant yeast system carrying the rainbow trout estrogen receptor

  12. Layer-by-layer structured polysaccharides-based multilayers on cellulose acetate membrane: Towards better hemocompatibility, antibacterial and antioxidant activities

    NASA Astrophysics Data System (ADS)

    Peng, Lincai; Li, Hui; Meng, Yahong

    2017-04-01

    The development of multifunctional cellulose acetate (CA) membranes with enhanced hemocompatibility and antibacterial and antioxidant activities is extremely important for biomedical applications. In this work, significant improvements in hemocompatibility and antibacterial and antioxidant activities of cellulose acetate (CA) membranes were achieved via layer-by-layer (LBL) deposition of chitosan (CS) and water-soluble heparin-mimicking polysaccharides (i.e., sulfated Cantharellus cibarius polysaccharides, SCP) onto their surface. The surface chemical compositions, growth manner, surface morphologies, and wetting ability of CS/SCP multilayer-modified CA membranes were characterized, respectively. The systematical evaluation of hemocompatibility revealed that CS/SCP multilayer-modified CA membranes significantly improved blood compatibility including resistance to non-specific protein adsorption, suppression of platelet adhesion and activation, prolongation of coagulation times, inhibition of complement activation, as well as reduction in blood hemolysis. Meanwhile, CS/SCP multilayer-modified CA membranes exhibited strong growth inhibition against Escherichia coli and Staphylococcus aureus, as well as high scavenging abilities against superoxide and hydroxyl radicals. In summary, the CS/SCP multilayers could confer CA membranes with integrated hemocompatibility and antibacterial and antioxidant activities, which might have great potential application in the biomedical field.

  13. FT-IR and Raman spectroscopic and DFT studies of anti-cancer active molecule N-{(meta-ferrocenyl) Benzoyl} - L-Alanine - Glycine ethyl ester

    NASA Astrophysics Data System (ADS)

    Xavier, T. S.; Kenny, Peter T. M.; Manimaran, D.; Joe, I. Hubert

    2015-06-01

    FT-Raman and FT-IR spectra of N-{(meta-ferrocenyl) Benzoyl} - L-alanine - glycine ethyl ester were recorded in solid phase. The optimized molecular geometry, the vibrational wavenumbers, the infrared intensities and the Raman scattering intensities were calculated by using density functional method(B3LYP) with 6-31G(d, p) basis set. Vibrational assignment of the molecule was done by using potential energy distribution analysis. Natural bond orbital analysis, Mulliken charge analysis and HOMO-LUMO energy were used to elucidate the reasons for intra molecular charge transfer. Docking studies were conducted to predict its anticancer activity.

  14. Influence of ovariohysterectomy and deslorelin acetate on the spontaneous activity of the rabbit urinary bladder in vitro.

    PubMed

    Bujok, Jolanta; Wincewicz, Edyta; Czerski, Albert; Zawadzki, Wojciech

    2016-02-01

    Lower urinary tract symptoms are not only a serious health problem but also a substantial sociologic issue affecting human beings and companion animals. Estrogen deficiency is considered an etiologic factor of urinary incontinence in postmenopausal women and spayed female dogs. However, insufficient effectiveness of hormonal therapy has caused an intensive search for new therapeutic options. GnRH analogs have positive clinical effects in neutered female dogs suffering from incontinence, but the mechanism of action is not known. The aim of our study was to determine the effect of long-acting deslorelin acetate on the spontaneous activity of urinary bladder sections from a rabbit model of long-term estrogen deprivation. The study was conducted on 21 female New Zealand White rabbits divided into the following groups: control group, ovariohysterectomized (OHX) group, and ovariohysterectomized group given a deslorelin acetate implant. Urinary bladders were excised immediately after sacrifice, and the spontaneous activity of dorsal and ventral strips of the bladder body was examined in organ bath chambers. The amplitude and frequency of the spontaneous contractions were evaluated. Most of the sections developed spontaneous activity. Ovariohysterectomy caused a decrease in the amplitude of spontaneous contractions of the tissues obtained only from the dorsal part of the bladder body. After OHX, the frequency was higher compared with the control group in both parts of the bladder. Deslorelin acetate did not significantly affect the spontaneous contraction amplitude but caused a decrease in the frequency in the dorsal and ventral parts of the bladder. In conclusion, long-term changes in the levels of hormones and other regulatory substances associated with the reproductive system are related to altered spontaneous activity of the urinary bladder, which may impact the symptoms of urgency and incontinence appearing in women after menopause and in female animals after

  15. Cardiomyocytes from phorbol myristate acetate-activated mesenchymal stem cells restore electromechanical function in infarcted rat hearts

    PubMed Central

    Song, Heesang; Hwang, Hye Jin; Chang, Woochul; Song, Byeong-Wook; Cha, Min-Ji; Lim, Soyeon; Choi, Eun Ju; Ham, Onju; Lee, Chang Youn; Park, Jun-Hee; Lee, Se-Yeon; Choi, Eunmi; Lee, Chungkeun; Lee, Myoungho; Lee, Moon-Hyoung; Kim, Sung-Hou; Jang, Yangsoo; Hwang, Ki-Chul

    2011-01-01

    Despite the safety and feasibility of mesenchymal stem cell (MSC) therapy, an optimal cell type has not yet emerged in terms of electromechanical integration in infarcted myocardium. We found that poor to moderate survival benefits of MSC-implanted rats were caused by incomplete electromechanical integration induced by tissue heterogeneity between myocytes and engrafted MSCs in the infarcted myocardium. Here, we report the development of cardiogenic cells from rat MSCs activated by phorbol myristate acetate, a PKC activator, that exhibited high expressions of cardiac-specific markers and Ca2+ homeostasis-related proteins and showed adrenergic receptor signaling by norepinephrine. Histological analysis showed high connexin 43 coupling, few inflammatory cells, and low fibrotic markers in myocardium implanted with these phorbol myristate acetate-activated MSCs. Infarct hearts implanted with these cells exhibited restoration of conduction velocity through decreased tissue heterogeneity and improved myocardial contractility. These findings have major implications for the development of better cell types for electromechanical integration of cell-based treatment for infarcted myocardium. PMID:21173226

  16. Antinociceptive activity of Maytenus rigida stem bark.

    PubMed

    Dias, Kellyane S; Marques, Maxsuel S; Menezes, Igor A C; Santos, Thiago C; Silva, Aline B L; Estevam, Charles S; Sant'Ana, Antônio E G; Pizza, Cosimo; Antoniolli, Angelo R; Marçal, Rosilene M

    2007-12-01

    Ethanol extract of Maytenus rigida stem bark and its fractions were assessed for antinociceptive activity in tail-flick test in rats. The activity was located in the chloroform, ethyl acetate and aq.methanol fractions. Phytochemical screening revealed that catechin was the only common class of compounds present on the ethanol extract as well as on the active fractions. 4'-Methylepigallocatechin, isolated from the ethyl acetate and aq.methanol fractions, showed antinociceptive effect in the tail-flick test (75 mg/kg; p.o.), which was reversed by the opiate antagonist naloxone (3 mg/kg; i.p.).

  17. Study of reactivity of cyanoacetohydrazonoethyl-N-ethyl-N-methyl benzenesulfonamide: preparation of novel anticancer and antimicrobial active heterocyclic benzenesulfonamide derivatives and their molecular docking against dihydrofolate reductase.

    PubMed

    Debbabi, Khaled F; Al-Harbi, Sami A; Al-Saidi, Hamed M; Aljuhani, Enas H; Abd El-Gilil, Shimaa M; Bashandy, Mahmoud S

    2016-01-01

    This article describes the synthesis of some novel heterocyclic sulfonamides having biologically active thiophene 3, 4, 5, 6, coumarin 8, benzocoumarin 9, thiazole 7, piperidine 10, pyrrolidine 11, pyrazole 14 and pyridine 12, 13. Starting with 4-(1-(2-(2-cyanoacetyl)hydrazono)ethyl)-N-ethyl-N-methylbenzenesulfonamide (2), which was prepared from condensation of acetophenone derivative 1 with 2-cyanoacetohydrazide. The structures of the newly synthesized compounds were confirmed by elemental analysis, IR, (1)H NMR, (13)C NMR, (19)F NMR and MS spectral data. All the newly synthesized heterocyclic sulfonamides were evaluated as in-vitro anti-breast cancer cell line (MCF7) and as in-vitro antimicrobial agents. Compounds 8, 5 and 11 were more active than MTX reference drug and compounds 12, 7, 4, 14, 5 and 8 were highly potent against Klebsiella pneumonia. Molecular operating environment performed virtual screening using molecular docking studies of the synthesized compounds. The results indicated that some prepared compounds are suitable inhibitor against dihydrofolate reductase (DHFR) enzyme (PDBSD:4DFR) with further modification.

  18. A novel polymer based on MtCu2+/cellulose acetate with antimicrobial activity.

    PubMed

    Bruna, J E; Galotto, M J; Guarda, A; Rodríguez, F

    2014-02-15

    Cellulose acetate (CA)/copper montmorillonite modified (MtCu(2+)) antimicrobial nanocomposites for food packaging containing 1, 3 and 5 wt.% nanoparticles were prepared by solution casting technique. X-ray diffraction (XRD) and transmission electron microscopy revealed the existence of intercalated and no intercalated clay form in the CA matrix. The thermal stability of the MtCu(2+)/CA nanocomposites was measured by TGA and DSC, which indicated that the nanocomposites were less thermally stable in comparison to CA pure. Mechanical testing of material did not show differences when MtCu(2+) was added in CA. On the other hand, antimicrobial effect was observed for nanocomposites films, obtaining a 98% reduction against Escherichia coli.

  19. Silver nanoparticles in combination with acetic acid and zinc oxide quantum dots for antibacterial activities improvement-A comparative study

    NASA Astrophysics Data System (ADS)

    Sedira, Sofiane; Ayachi, Ahmed Abdelhakim; Lakehal, Sihem; Fateh, Merouane; Achour, Slimane

    2014-08-01

    Due to their remarkable antibacterial/antivirus properties, silver nanoparticles (Ag NPs) and zinc oxide quantum dots (ZnO Qds) have been widely used in the antimicrobial field. The mechanism of action of Ag NPs on bacteria was recently studied and it has been proven that Ag NPs exerts their antibacterial activities mainly by the released Ag+. In this work, Ag NPs and ZnO Qds were synthesized using polyol and hydrothermal method, respectively. It was demonstrated that Ag NPs can be oxidized easily in aqueous solution and the addition of acetic acid can increase the Ag+ release which improves the antibacterial activity of Ag NPs. A comparative study between bactericidal effect of Ag NPs/acetic acid and Ag NPs/ZnO Qds on Pseudomonas aeruginosa, Escherichia coli, Klebsiella pneumonia and Staphylococcus aureus was undertaken using agar diffusion method. The obtained colloids were characterized using UV-vis spectroscopy, Raman spectrometry, X-ray diffraction (XRD), transmission electron microscopy (TEM) and atomic force microscopy (AFM).

  20. Influence of iron solubility and charged surface-active compounds on lipid oxidation in fatty acid ethyl esters containing association colloids.

    PubMed

    Homma, Rika; Johnson, David R; McClements, D Julian; Decker, Eric A

    2016-05-15

    The impact of iron compounds with different solubilities on lipid oxidation was studied in the presence and absence of association colloids. Iron (III) sulfate only accelerated lipid oxidation in the presence of association colloids while iron (III) oleate accelerated oxidation in the presence and absence of association colloids. Further, iron (III) oxide retarded lipid oxidation both with and without association colloids. The impact of charged association colloids on lipid oxidation in ethyl oleate was also investigated. Association colloids consisting of the anionic surface-active compound dodecyl sulphosuccinate sodium salt (AOT), cationic surface-active compound hexadecyltrimethylammonium bromide (CTAB), and nonionic surface-active compound 4-(1,1,3,3-tetramethylbutyl)phenyl-polyethylene glycol (Triton X-100) retarded, promoted, and had no effect on lipid oxidation rates, respectively. These results indicate that the polarity of metal compounds and the charge of association colloids play a big role in lipid oxidation.

  1. Structure--activity relationship and mode of action of N-(6-ferrocenyl-2-naphthoyl) dipeptide ethyl esters: novel organometallic anticancer compounds.

    PubMed

    Mooney, Aine; Tiedt, Rachel; Maghoub, Thamir; O'Donovan, Norma; Crown, John; White, Blánaid; Kenny, Peter T M

    2012-06-14

    In this article, we report the findings of a comprehensive structure-activity relationship study of N-(6-ferrocenyl-2-naphthoyl) dipeptide ethyl esters, in which novel analogues were designed, synthesized, and evaluated in vitro for antiproliferative effect. Two new compounds, 2 and 16, showed potent nanomolar activity in the H1299 NSCLC cell line, with exceptional IC(50) values of 0.13 and 0.14 μM, respectively. These compounds were also found to have significant activity in the Sk-Mel-28 malignant melanoma cell line (IC(50) values of 1.10 and 1.06 μM, respectively). Studies were also conducted to elucidate the mode of action of these novel organometallic anticancer compounds. Cell cycle analysis in the H1299 cell line suggests these compounds induce apoptosis, while guanine oxidation studies confirm that 2 is capable of generating oxidative damage via a ROS-mediated mechanism.

  2. Modification of the photocatalytic activity of TiO2 by β-Cyclodextrin in decoloration of ethyl violet dye

    PubMed Central

    Velusamy, Ponnusamy; Pitchaimuthu, Sakthivel; Rajalakshmi, Subramanian; Kannan, Nagarathinam

    2012-01-01

    The photocatalytic decoloration of an organic dye, ethyl violet (EV), has been studied in the presence of TiO2 and the addition of β-Cyclodextrin (β-CD) with TiO2 (TiO2-β-CD) under UV-A light irradiation. The different operating parameters like initial concentration of dye, illumination time, pH and amount of catalyst used have also been investigated. The photocatalytic decoloration efficiency is more in the TiO2-β-CD/UV-A light system than TiO2/UV-A light system. The mineralization of EV has been confirmed by Chemical Oxygen Demand (COD) measurements. The complexation patterns have been confirmed with UV–Visible and FT-IR spectral data and the interaction between TiO2 and β-CD have been characterized by powder XRD analysis and UV–Visible diffuse reflectance spectroscopy. PMID:25685468

  3. Activity Coefficients at Infinite Dilution and Physicochemical Properties for Organic Solutes and Water in the Ionic Liquid 1-Ethyl-3-methylimidazolium trifluorotris(perfluoroethyl)phosphate.

    PubMed

    Wlazło, Michał; Marciniak, Andrzej; Letcher, Trevor M

    New data of activity coefficients at infinite dilution, γ13(∞), for 65 different solutes including alkanes, alkenes, alkynes, cycloalkanes, aromatic hydrocarbons, alcohols, thiophene, ethers, ketones, aldehydes, esters and water in the ionic liquid 1-ethyl-3-methylimidazolium trifluorotris(perfluoroethyl)phosphate, were determined using inverse gas chromatography within the temperature range from 318.15 to 368.15 K. This is a continuation of our study of ionic liquids based on this anion. The results are compared with the other trifluorotris(perfluoroethyl)phosphate ionic liquids. The γ13(∞) values were used to calculate thermodynamic functions such as partial molar excess Gibbs energies [Formula: see text], enthalpies [Formula: see text] and entropies [Formula: see text] as well as gas-liquid partition coefficients of the solutes, KL. These values were used to determine the linear free energy relationship (LFER) system constants as a function of temperature. The selectivities at infinite dilution needed for some extraction problems were calculated and compared with literature data of ionic liquids based on the trifluorotris(perfluoroethyl)phosphate anion and the 1-ethyl-3-methylimidazolium cation. Additionally, the density and viscosity of the investigated ionic liquid at temperatures from 298.15 to 348.15 K were measured.

  4. Chitosan acetate as an active coating material and its effects on the storing of Prunus avium L.

    PubMed

    Dang, Qi Feng; Yan, Jing Quan; Li, Yan; Cheng, Xiao Jie; Liu, Cheng Sheng; Chen, Xi Guang

    2010-03-01

    In this article, chitosan acetate (CA) was prepared by the method of solid-liquid reaction. CA was a stable faint yellow powder with water solubility. CA kept the same backbone in the chemical structure as the raw material of chitosan, and it also had the similar antibacterial properties with chitosan. CA could form a coating film on the outside surface of the sweet cherries, could effectively retard the loss of the water, titratable acidity, and ascorbic acid of sweet cherries, and could induce a significant increase in the peroxidase and catalase activities in the fruit. The CA coating could also increase the ratio of the total soluble solids and titratable acidity in the fruit. The application of CA effectively maintained quality attributes and extended postharvest life of the sweet cherries. The results revealed that the CA salts had potential application in active edible coating materials in the storage of fresh fruit.

  5. Thallium acetate

    Integrated Risk Information System (IRIS)

    Jump to main content . Integrated Risk Information System Recent Additions | Contact Us Search : All EPA IRIS • You are here : EPA Home • Research • Environmental Assessment • IRIS • IRIS Summaries Redirect Page As of September 30 , 2009 , the assessment summary for Thallium acetate is included in t

  6. Phenylmercuric acetate

    Integrated Risk Information System (IRIS)

    Phenylmercuric acetate ; CASRN 62 - 38 - 4 Human health assessment information on a chemical substance is included in the IRIS database only after a comprehensive review of toxicity data , as outlined in the IRIS assessment development process . Sections I ( Health Hazard Assessments for Noncarcinog

  7. Ammonium acetate

    Integrated Risk Information System (IRIS)

    Ammonium acetate ; CASRN 631 - 61 - 8 Human health assessment information on a chemical substance is included in the IRIS database only after a comprehensive review of toxicity data , as outlined in the IRIS assessment development process . Sections I ( Health Hazard Assessments for Noncarcinogenic

  8. Vinyl acetate

    Integrated Risk Information System (IRIS)

    Vinyl acetate ; CASRN 108 - 05 - 4 Human health assessment information on a chemical substance is included in the IRIS database only after a comprehensive review of toxicity data , as outlined in the IRIS assessment development process . Sections I ( Health Hazard Assessments for Noncarcinogenic Eff

  9. Subacute Exposure to N-Ethyl Perfluorooctanesulfonamidoethanol Results in the Formation of Perfluorooctanesulfonate and Alters Superoxide Dismutase Activity in Female Rats

    PubMed Central

    Xie, Wei; Wu, Qian; Kania-Korwel, Izabela; Tharappel, Job C.; Telu, Sanjay; Coleman, Mitchell C.; Glauert, Howard P.; Kannan, Kurunthachalam; Santhana Mariappan, S. V.; Spitz, Douglas R.; Weydert, Jamie; Lehmler, Hans-Joachim

    2009-01-01

    Perfluorooctanesulfonamides, such as N-ethyl perfluorooctanesulfonamidoethanol (N-EtFOSE), are large scale industrial chemicals but their disposition and toxicity are poorly understood despite significant human exposure. The hypothesis that subacute exposure to N-EtFOSE, a weak peroxisome proliferator, causes a redox imbalance in vivo was tested using the known peroxisome proliferator, ciprofibrate, as a positive control. Female Sprague-Dawley rats were treated orally with N-EtFOSE, ciprofibrate or corn oil (vehicle) for 21 days, and levels of N-EtFOSE and its metabolites as well as markers of peroxisome proliferation and oxidative stress were assessed in serum, liver and/or uterus. The N-EtFOSE metabolite profile in liver and serum was in good agreement with reported in vitro biotransformation pathways in rats and the metabolite levels decreasing in the order perfluorooctanesulfonate ≫ perfluorooctanesulfonamide ∼ N-ethyl perfluorooctanesulfonamidoacetate ≫ perfluorooctanesulfonamidoethanol ∼ N-EtFOSE. Although N-EtFOSE treatment significantly decreased the growth rate, increased relative liver weight and activity of superoxide dismutases (SOD) in liver and uterus (total SOD, CuZnSOD and MnSOD), a metabolic study revealed no differences in the metabolome in serum from N-EtFOSE-treated and control animals. Ciprofibrate treatment increased liver weight and peroxisomal acyl Co-A oxidase activity in the liver and altered antioxidant enzyme activities in the uterus and liver. According to NMR metabolomic studies, ciprofibrate treated animals had altered serum lipid profiles compared to N-EtFOSE-treated and control animals, whereas putative markers of peroxisome proliferation in serum were not affected. Overall, this study demonstrates the biotransformation of N-EtFOSE to PFOS in rats that is accompanied by N-EtFOSE-induced alterations in antioxidant enzyme activity. PMID:19544052

  10. Dactyloditerpenol acetate, a new prenylbisabolane-type diterpene from Aplysia dactylomela with significant in vitro anti-neuroinflammatory activity.

    PubMed

    Jiménez-Romero, Carlos; Mayer, Alejandro M S; Rodríguez, Abimael D

    2014-01-01

    A new regular diterpene possessing an unusual 1,6-anti-3-methylcyclohex-2-en-1-ol ring system, dactyloditerpenol acetate (1), has been extracted from the tropical sea hare Aplysia dactylomela and its stereostructure elucidated by spectroscopic methods. The absolute configuration of 1 was determined as 1S, 6S, 7R, 10S, and 11R by application of Kishi's method for the assignment of absolute configuration of alcohols. The new diterpene potently inhibited in vitro thromboxane B2 (TXB2) (IC50 0.4μM) and superoxide anion (O2(-)) (IC50 1μM) generation from Escherichia coli lipopolysaccharide (LPS)-activated rat neonatal microglia, with concomitant low short-term toxicity.

  11. N-(2-(arylmethylimino)ethyl)-7-chloroquinolin-4-amine derivatives, synthesized by thermal and ultrasonic means, are endowed with anti-Zika virus activity.

    PubMed

    Barbosa-Lima, Giselle; da Silveira Pinto, Ligia S; Kaiser, Carlos R; Wardell, James L; De Freitas, Caroline S; Vieira, Yasmine R; Marttorelli, Andressa; Cerbino Neto, José; Bozza, Patrícia T; Wardell, Solange M S V; de Souza, Marcus V N; Souza, Thiago M L

    2017-02-15

    Zika virus (ZIKV), an emerging Flavivirus, was recently associated with severe neurological complications and congenital diseases. Therefore, development of antiviral agents capable of inhibiting ZIKV replication is urgent. Chloroquine is a molecule with a confirmed safety history for use with pregnant women, and has been found to exhibit anti-ZIKV activity at concentrations around 10 μM. This suggests that modifications to the chloroquine structure could be promising for obtaining more effective anti-ZIKV agents. Here, we report the ability of a series of N-(2-(arylmethylimino)ethyl)-7-chloroquinolin-4-amine derivatives to inhibit ZIKV replication in vitro. We have found that the quinoline derivative, N-(2-((5-nitrofuran-2-yl)methylimino)ethyl)-7-chloroquinolin-4-amine, 40, was the most potent compound within this series, reducing ZIKV replication by 72% at 10 μM. Compound 40 exhibits an EC50 value of 0.8 ± 0.07 μM, compared to that of chloroquine of 12 ± 3.2 μM. Good activities were also obtained for other compounds, including those with aryl groups = phenyl, 4-fluorophenyl, 4-nitrophenyl, 2,6-dimethoxyphenyl, 3-pyridinyl and 5-nitrothien-2-yl. Syntheses of these quinoline derivatives have been obtained both by thermal and ultrasonic means. The ultrasonic method produced comparable yields to the thermal (reflux) method in very much shorter times 30-180 s compared to 30-180 min reactions times. These results indicate that this group of compounds is a good follow-up point for the potential discovery of new drugs against the Zika disease.

  12. Lewis base activation of Lewis acids: catalytic, enantioselective addition of glycolate-derived silyl ketene acetals to aldehydes.

    PubMed

    Denmark, Scott E; Chung, Won-Jin

    2008-06-20

    A catalytic system involving silicon tetrachloride and a chiral, Lewis basic bisphosphoramide catalyst is effective for the addition of glycolate-derived silyl ketene acetals to aldehydes. It was found that the sense of diastereoselectivity could be modulated by changing the size of the substituents on the silyl ketene acetals. In general, the trimethylsilyl ketene acetals derived from methyl glycolates with a large protecting group on the alpha-oxygen provide enantiomerically enriched alpha,beta-dihydroxy esters with high syn-diastereoselectivity, whereas the tert-butyldimethylsilyl ketene acetals derived from bulky esters of alpha-methoxyacetic acid provide enantiomerically enriched alpha,beta-dihydroxy esters with high anti-diastereoselecitvity.

  13. Ethyl 2-{(2Z)-2-[(1-naphthyl­sulfon­yl)imino]-2,3-dihydro-1,3-thia­zol-4-yl}acetate monohydrate

    PubMed Central

    Navarrete-Vázquez, Gabriel; Morales-Vilchis, Guadalupe; Estrada-Soto, Samuel; Rodríguez-López, Verónica; Tlahuext, Hugo

    2010-01-01

    The title compound, C17H16N2O4S2·H2O, is of inter­est with respect to its anti­diabetic and anti-obesity activity. In the crystal, the packing is stabilized by three cooperative inter­actions: offset π–π inter­actions [centroid–centroid distance = 3.604 (2) Å], as well as C—H⋯O and O—H⋯O hydrogen bonds. N—H⋯O inter­actions also occur. PMID:21588949

  14. Sodium [2'-[(cyclopropanecarbonyl-ethyl-amino)-methyl]-4'-(6-ethoxy-pyridin-3-yl)-6-methoxy-biphenyl-3-yl]-acetate (AM432): a potent, selective prostaglandin D2 receptor antagonist.

    PubMed

    Stock, Nicholas; Volkots, Deborah; Stebbins, Karin; Broadhead, Alex; Stearns, Brian; Roppe, Jeffrey; Parr, Timothy; Baccei, Christopher; Bain, Gretchen; Chapman, Charles; Correa, Lucia; Darlington, Janice; King, Christopher; Lee, Catherine; Lorrain, Daniel S; Prodanovich, Pat; Santini, Angelina; Evans, Jilly F; Hutchinson, John H; Prasit, Peppi

    2011-02-01

    Compound 21 (AM432) was identified as a potent and selective antagonist of the DP(2) receptor (CRTH2). Modification of a bi-aryl core identified a series of tri-aryl antagonists of which compound 21 proved a viable clinical candidate. AM432 shows excellent potency in a human whole blood eosinophil shape change assay with prolonged incubation, a comparatively long off-rate from the DP(2) receptor, excellent pharmacokinetics in dog and in vivo activity in two mouse models of inflammatory disease after oral dosing.

  15. Tuning Chocolate Flavor through Development of Thermotolerant Saccharomyces cerevisiae Starter Cultures with Increased Acetate Ester Production.

    PubMed

    Meersman, Esther; Steensels, Jan; Struyf, Nore; Paulus, Tinneke; Saels, Veerle; Mathawan, Melissa; Allegaert, Leen; Vrancken, Gino; Verstrepen, Kevin J

    2015-11-20

    Microbial starter cultures have extensively been used to enhance the consistency and efficiency of industrial fermentations. Despite the advantages of such controlled fermentations, the fermentation involved in the production of chocolate is still a spontaneous process that relies on the natural microbiota at cocoa farms. However, recent studies indicate that certain thermotolerant Saccharomyces cerevisiae cultures can be used as starter cultures for cocoa pulp fermentation. In this study, we investigate the potential of specifically developed starter cultures to modulate chocolate aroma. Specifically, we developed several new S. cerevisiae hybrids that combine thermotolerance and efficient cocoa pulp fermentation with a high production of volatile flavor-active esters. In addition, we investigated the potential of two strains of two non-Saccharomyces species that produce very large amounts of fruity esters (Pichia kluyveri and Cyberlindnera fabianii) to modulate chocolate aroma. Gas chromatography-mass spectrometry (GC-MS) analysis of the cocoa liquor revealed an increased concentration of various flavor-active esters and a decrease in spoilage-related off-flavors in batches inoculated with S. cerevisiae starter cultures and, to a lesser extent, in batches inoculated with P. kluyveri and Cyb. fabianii. Additionally, GC-MS analysis of chocolate samples revealed that while most short-chain esters evaporated during conching, longer and more-fat-soluble ethyl and acetate esters, such as ethyl octanoate, phenylethyl acetate, ethyl phenylacetate, ethyl decanoate, and ethyl dodecanoate, remained almost unaffected. Sensory analysis by an expert panel confirmed significant differences in the aromas of chocolates produced with different starter cultures. Together, these results show that the selection of different yeast cultures opens novel avenues for modulating chocolate flavor.

  16. Tuning Chocolate Flavor through Development of Thermotolerant Saccharomyces cerevisiae Starter Cultures with Increased Acetate Ester Production

    PubMed Central

    Meersman, Esther; Steensels, Jan; Struyf, Nore; Paulus, Tinneke; Saels, Veerle; Mathawan, Melissa; Allegaert, Leen; Vrancken, Gino

    2015-01-01

    Microbial starter cultures have extensively been used to enhance the consistency and efficiency of industrial fermentations. Despite the advantages of such controlled fermentations, the fermentation involved in the production of chocolate is still a spontaneous process that relies on the natural microbiota at cocoa farms. However, recent studies indicate that certain thermotolerant Saccharomyces cerevisiae cultures can be used as starter cultures for cocoa pulp fermentation. In this study, we investigate the potential of specifically developed starter cultures to modulate chocolate aroma. Specifically, we developed several new S. cerevisiae hybrids that combine thermotolerance and efficient cocoa pulp fermentation with a high production of volatile flavor-active esters. In addition, we investigated the potential of two strains of two non-Saccharomyces species that produce very large amounts of fruity esters (Pichia kluyveri and Cyberlindnera fabianii) to modulate chocolate aroma. Gas chromatography-mass spectrometry (GC-MS) analysis of the cocoa liquor revealed an increased concentration of various flavor-active esters and a decrease in spoilage-related off-flavors in batches inoculated with S. cerevisiae starter cultures and, to a lesser extent, in batches inoculated with P. kluyveri and Cyb. fabianii. Additionally, GC-MS analysis of chocolate samples revealed that while most short-chain esters evaporated during conching, longer and more-fat-soluble ethyl and acetate esters, such as ethyl octanoate, phenylethyl acetate, ethyl phenylacetate, ethyl decanoate, and ethyl dodecanoate, remained almost unaffected. Sensory analysis by an expert panel confirmed significant differences in the aromas of chocolates produced with different starter cultures. Together, these results show that the selection of different yeast cultures opens novel avenues for modulating chocolate flavor. PMID:26590272

  17. Helenalin Acetate, a Natural Sesquiterpene Lactone with Anti-inflammatory and Anti-cancer Activity, Disrupts the Cooperation of CCAAT Box/Enhancer-binding Protein β (C/EBPβ) and Co-activator p300.

    PubMed

    Jakobs, Anke; Steinmann, Simone; Henrich, Sarah Marie; Schmidt, Thomas J; Klempnauer, Karl-Heinz

    2016-12-09

    Recent work has demonstrated pro-oncogenic functions of the transcription factor CCAAT box/enhancer-binding protein β (C/EBPβ) in various tumors, implicating C/EBPβ as an interesting target for the development of small-molecule inhibitors. We have previously discovered that the sesquiterpene lactone helenalin acetate, a natural compound known to inhibit NF-κB, is a potent C/EBPβ inhibitor. We have now examined the inhibitory mechanism of helenalin acetate in more detail. We demonstrate that helenalin acetate is a significantly more potent inhibitor of C/EBPβ than of NF-κB. Our work shows that helenalin acetate inhibits C/EBPβ by binding to the N-terminal part of C/EBPβ, thereby disrupting the cooperation of C/EBPβ with the co-activator p300. C/EBPβ is expressed in several isoforms from alternative translational start codons. We have previously demonstrated that helenalin acetate selectively inhibits only the full-length (liver-enriched activating protein* (LAP*)) isoform but not the slightly shorter (LAP) isoform. Consistent with this, helenalin acetate binds to the LAP* but not to the LAP isoform, explaining why its inhibitory activity is selective for LAP*. Although helenalin acetate contains reactive groups that are able to interact covalently with cysteine residues, as exemplified by its effect on NF-κB, the inhibition of C/EBPβ by helenalin acetate is not due to irreversible reaction with cysteine residues of C/EBPβ. In summary, helenalin acetate is the first highly active small-molecule C/EBPβ inhibitor that inhibits C/EBPβ by a direct binding mechanism. Its selectivity for the LAP* isoform also makes helenalin acetate an interesting tool to dissect the functions of the LAP* and LAP isoforms.

  18. Glatiramer acetate attenuates the activation of CD4+ T cells by modulating STAT1 and −3 signaling in glia

    PubMed Central

    Ahn, Ye-Hyeon; Jeon, Sae-Bom; Chang, Chi Young; Goh, Eun-Ah; Kim, Sang Soo; Kim, Ho Jin; Song, Jaewhan; Park, Eun Jung

    2017-01-01

    Interactions between immune effector cells of the central nervous system appear to directly or indirectly influence the progress/regression of multiple sclerosis (MS). Here, we report that glial STAT1 and −3 are distinctively phosphorylated following the interaction of activated lymphocytes and glia, and this effect is significantly inhibited by glatiramer acetate (GA), a disease-modifying drug for MS. GA also reduces the activations of STAT1 and −3 by MS-associated stimuli such as IFNγ or LPS in primary glia, but not neurons. Experiments in IFNγ- and IFNγ receptor-deficient mice revealed that GA-induced inhibitions of STAT signaling are independent of IFNγ and its receptor. Interestingly, GA induces the expression levels of suppressor of cytokine signaling-1 and −3, representative negative regulators of STAT signaling in glia. We further found that GA attenuates the LPS-triggered enhancement of IL-2, a highly produced cytokine in patients with active MS, in CD4+ T cells co-cultured with glia, but not in CD4+ T cells alone. Collectively, these results provide that activation of glial STATs is an essential event in the interaction between glia and T cells, which is a possible underlying mechanism of GA action in MS. These findings provide an insight for the development of targeted therapies against MS. PMID:28094337

  19. Molluscicidal activity of some Moroccan medicinal plants.

    PubMed

    Hmamouchi, M; Lahlou, M; Agoumi, A

    2000-06-01

    Among 14 plants of Moroccan folk medicine tested for molluscicidal activity, ethyl acetate extract from Origanum compactum and hexane extracts from both Chenopodium ambrosioides and Ruta chalepensis were the most active (LC(90)=2.00, 2.23 and 2.23 mg l(-1), respectively) against the schistosomiasis-transmitting snail Bulinus truncatus.

  20. In vitro antibacterial and cytotoxic activities of different parts of plant Swietenia mahagony.

    PubMed

    Haque, M; Ullah, M Obayed; Nahar, K

    2009-04-01

    Crude extracts from different parts (leaf, bark and seed) of Swietenia mahagony (Family: Meliaceae) were screened for their antibacterial activity against 4 Gram positive and 8 Gram negative bacteria. Disc diffusion technique was used for in vitro screening. Among the crude extracts, chloroform and ethyl acetate extracts of leaf and bark showed good activity against all the tested organisms. The chloroform and ethyl acetate extracts of seed exhibited little or positive effect against most of the tested bacteria. The activities were compared to a standard antibiotic-kanamycin. Cytotoxic activity of crude extracts were determined using brine shrimp lethality bioassay and standard vincristine sulphate was used as positive control. The chloroform extract of seed and ethyl acetate extract of bark showed good cytotoxic activities and the LC50 values were found 13.75 and 11.64 microg mL(-1), respectively.

  1. Ethyl acetate fraction of Garcina epunctata induces apoptosis in human promyelocytic cells (HL-60) through the ROS generation and G0/G1 cell cycle arrest: a bioassay-guided approach.

    PubMed

    Constant Anatole, Pieme; Guru, Santoh Kumar; Bathelemy, Ngamegni; Jeanne, Ngogang; Bhushan, Shashi; Murayama, Tetsuya; Saxena, Ajit Kumar

    2013-11-01

    Number of deaths due to cancer diseases is increasing in the world. There is an urgent need to develop alternative therapeutic measures against the disease. Our study reports the cytotoxicity activity of Garcina epunctata (gutifferae) in human promyelocytic leukemia cells (HL-60) and prostate cancer cells (PC-3) was evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT). Changes in mitochondrial membrane potential (MMP), reactive oxygen species (ROS) and morphological changes associated with apoptosis were examined by flow cytometry and Hoescht staining respectively. The results of in vitro antiproliferative screening of fractions and extract from G. epunctata indicated that three fractions inhibited the viability of PC-3 cells with IC₅₀ varied from 50 to 88 μ/ml while two fractions inhibited the proliferation of HL-60 cells with IC₅₀ range between 47.5 and 12 μg/ml. Among the entire fraction tested, Hex-EtOAc (75:25) showed cytotoxic effects on the two cell lines and EtOAc fraction was most active only HL-60 cells (12 μg/ml). Treatment of HL-60 cells with G. epunctata (20, 50, 100 μg/ml) for 24 h led to a significant dose-dependent increase in the percentage of cells in sub-G1 phase by analysis of the content of DNA in cells, and a number of apoptotic bodies containing nuclear fragments were observed in cells treated with 100 μg/ml. The EtOAc fraction of G. epunctata treatment significantly arrested HL-60 cells at the G0/G1 phase (p<0.05) and ROS was significantly elevated as well as the loss of membrane mitochondrial potential in a concentration dependant manner. The results demonstrated that the EtOAc fraction of G. epunctata inhibited the proliferation of HL-60 cells, leading to cell cycle arrest and programmed cell death, which was confirmed to occur through the mitochondrial pathway.

  2. Improvement in enzyme activity and stability by addition of low molecular weight polyethylene glycol to sodium bis(2-ethyl-L-hexyl)sulfosuccinate/isooctane reverse micellar system.

    PubMed

    Talukder, M M R; Takeyama, T; Hayashi, Y; Wu, J C; Kawanishi, T; Shimizu, N; Ogino, C

    2003-08-01

    The activity and stability of Chromobacterium viscosum lipase (glycerolester hydrolase, EC 3.1.1.3)-catalyzed olive oil hydrolysis in sodium bis (2-ethyl-l-hexyl)sulfosuccinate (AOT)/isooctane reverse micelles is increased appreciably when low molecular weight polyethylene glycol (PEG 400) is added to the reverse micelles. To understand the effect of PEG 400 on the phase behavior of the reverse micellar system, the phase diagram of AOT/ PEG 400/water/isooctane system was studied. The influences of relevant parameters on the catalytic activity in AOT/PEG 400 reverse micelles were investigated and compared with the results in the simple AOT reverse micelles. In the presence of PEG 400, the linear decreasing trend of the lipase activity with AOT concentration, which is observed in the simple AOT reverse micelles, disappeared. Enzyme entrapped in AOT/PEG reverse micelles was very stable, retaining >75% of its initial activity after 60 d, whereas the half-life in simple AOT reverse micelles was 38 d. The kinetics parameter maximum velocity (Vmax) exhibiting the temperature dependence and the activation energy obtained by Arrhenius plot was suppressed significantly by the addition of PEG 400.

  3. The antibacterial activity of chloroxylenol in combination with ethylenediaminetetra-acetic acid.

    PubMed Central

    Dankert, J.; Schut, I. K.

    1976-01-01

    The bactericidal activity of RBA 777 has been found to vary with both the cultural and environmental test conditions against Pseudomonas aeruginosa and to a lesser extent against Staphylococcus aureus. These variations may explain certain anomalies in earlier work regarding the activity of chloroxylenol-based products. The addition of EDTA to RBA 777 has brought about an improvement in the performance against P. aeruginosa and this activity is confirmed in vivo. Previous reports have already illustrated this potential and the evaluations of the new antibacterial agent DA 136 confirms and extends these results to its performance under adverse conditions, often associated with the hospital environment. PMID:812899

  4. The antibacterial activity of chloroxylenol in combination with ethylenediaminetetra-acetic acid.

    PubMed

    Dankert, J; Schut, I K

    1976-02-01

    The bactericidal activity of RBA 777 has been found to vary with both the cultural and environmental test conditions against Pseudomonas aeruginosa and to a lesser extent against Staphylococcus aureus. These variations may explain certain anomalies in earlier work regarding the activity of chloroxylenol-based products. The addition of EDTA to RBA 777 has brought about an improvement in the performance against P. aeruginosa and this activity is confirmed in vivo. Previous reports have already illustrated this potential and the evaluations of the new antibacterial agent DA 136 confirms and extends these results to its performance under adverse conditions, often associated with the hospital environment.

  5. The metabolic activation and nucleic acid adducts of naturally-occurring carcinogens: recent results with ethyl carbamate and the spice flavors safrole and estragole.

    PubMed Central

    Miller, J. A.; Miller, E. C.

    1983-01-01

    A small (approximately 30) but varied group of organic and inorganic compounds appear to be carcinogenic in both humans and experimental animals. A much larger number and wider variety of chemical carcinogens, primarily synthetic organic compounds, are known for experimental animals. These agents include a small (approximately 30) and varied group of metabolites of green plants and fungi. Many more of these carcinogens must exist in the living world. As with the synthetic carcinogens, the majority of these naturally occurring carcinogens are procarcinogens that require metabolic conversion into reactive electrophilic and mutagenic ultimate carcinogens. These strong electrophiles combine covalently and non-enzymatically with nucleophilic sites in DNAs, RNAs, proteins, and small molecules in target tissues. One or more of the DNA adducts appear to initiate carcinogenesis in an irreversible manner. The subsequent promotion step leading to gross tumours may be completed by further administration of carcinogen or by treatment with non-carcinogenic promoters. Roles for the RNA and protein adducts in the carcinogenic process have not been excluded. Recent data on the metabolic activation and reactivity in vivo of the naturally occurring carcinogens ethyl carbamate and certain of the alkenylbenzene spice flavours are illustrative of these principles. These agents can initiate the carcinogenic process in male mouse liver with small doses given prior to weaning. Subsequent growth of the liver and male hormonal factors appear to function as promoters leading to gross hepatic tumors after one year. Reactive electrophilic metabolites of ethyl carbamate and of safrole and estragole and their nucleic acid adducts formed during initiation in mouse liver have been characterized. PMID:6191767

  6. Rhodium-Catalyzed β-Selective Oxidative Heck-Type Coupling of Vinyl Acetate via C-H Activation.

    PubMed

    Zhang, Hui-Jun; Lin, Weidong; Su, Feng; Wen, Ting-Bin

    2016-12-16

    An efficient Rh(III)-catalyzed direct ortho-C-H olefination of acetanilides with vinyl acetate was developed. This protocol provides a straightforward pathway to a series of (E)-2-acetamidostyryl acetates, giving access to indole derivatives following a simple hydrolysis/cyclization process.

  7. Generation of poly-β-hydroxybutyrate from acetate in higher plants: Detection of acetoacetyl CoA reductase- and PHB synthase- activities in rice.

    PubMed

    Tsuda, Hirohisa; Shiraki, Mari; Inoue, Eri; Saito, Terumi

    2016-08-20

    It has been reported that Poly-β-hydroxybutyrate (PHB) is generated from acetate in the rice root. However, no information is available about the biosynthetic pathway of PHB from acetate in plant cells. In the bacterium Ralstonia eutropha H16 (R. eutropha), PHB is synthesized from acetyl CoA by the consecutive reaction of three enzymes: β-ketothiolase (EC: 2.3.1.9), acetoacetyl CoA reductase (EC: 1.1.1.36) and PHB synthase (EC: 2.3.1.-). Thus, in this study, we examined whether the above three enzymatic activities were also detected in rice seedlings. The results clearly showed that the activities of the above three enzymes were all detected in rice. In particular, the PHB synthase activity was detected specifically in the sonicated particulate fractions (2000g 10min precipitate (ppt) and the 8000g 30min ppt) of rice roots and leaves. In addition to these enzyme activities, several new experimental results were obtained on PHB synthesis in higher plants: (a) (14)C-PHB generated from 2-(14)C-acetate was mainly localized in the 2000g 10min ppt and the 8000g 30min ppt of rice root. (b) Addition of acetate (0.1-10mM) to culture medium of rice seedlings did not increase the content of PHB in the rice root or leaf. (c) In addition to C3 plants, PHB was generated from acetate in a C4 plant (corn) and in a CAM plant (Bryophyllum pinnatum). d) Washing with ethylenediaminetetraacetic acid (EDTA) strongly suggested that the PHB synthesized from acetate was of plant origin and was not bacterial contamination.

  8. Enzyme activity in dialkyl phosphate ionic liquids

    SciTech Connect

    Thomas, M.F.; Dunn, J.; Li, L.-L.; Handley-Pendleton, J. M.; van der lelie, D.; Wishart, J. F.

    2011-12-01

    The activity of four metagenomic enzymes and an enzyme cloned from the straw mushroom, Volvariellavolvacea were studied in the following ionic liquids, 1,3-dimethylimidazolium dimethyl phosphate, [mmim][dmp], 1-ethyl-3-methylimidazolium dimethyl phosphate, [emim][dmp], 1-ethyl-3-methylimidazolium diethyl phosphate, [emim][dep] and 1-ethyl-3-methylimidazolium acetate, [emim][OAc]. Activity was determined by analyzing the hydrolysis of para-nitrobenzene carbohydrate derivatives. In general, the enzymes were most active in the dimethyl phosphate ionic liquids, followed by acetate. Generally speaking, activity decreased sharply for concentrations of [emim][dep] above 10% v/v, while the other ionic liquids showed less impact on activity up to 20% v/v.

  9. Experimental and computational investigation of acetic acid deoxygenation over oxophilic molybdenum carbide: Surface chemistry and active site identity

    SciTech Connect

    Schaidle, Joshua A.; Blackburn, Jeffrey; Farberow, Carrie A.; Nash, Connor; Steirer, K. Xerxes; Clark, Jared; Robichaud, David J.; Ruddy, Daniel A.

    2016-01-21

    Ex situ catalytic fast pyrolysis (CFP) is a promising route for producing fungible biofuels; however, this process requires bifunctional catalysts that favor C–O bond cleavage, activate hydrogen at near atmospheric pressure and high temperature (350–500 °C), and are stable under high-steam, low hydrogen-to-carbon environments. Recently, early transition-metal carbides have been reported to selectively cleave C–O bonds of alcohols, aldehydes, and oxygenated aromatics, yet there is limited understanding of the metal carbide surface chemistry under reaction conditions and the identity of the active sites for deoxygenation. In this study, we evaluated molybdenum carbide (Mo2C) for the deoxygenation of acetic acid, an abundant component of biomass pyrolysis vapors, under ex situ CFP conditions, and we probed the Mo2C surface chemistry, identity of the active sites, and deoxygenation pathways using in situ diffuse reflectance infrared Fourier transform spectroscopy (DRIFTS), X-ray photoelectron spectroscopy (XPS), and density functional theory (DFT) calculations.

  10. Experimental and computational investigation of acetic acid deoxygenation over oxophilic molybdenum carbide: Surface chemistry and active site identity

    DOE PAGES

    Schaidle, Joshua A.; Blackburn, Jeffrey; Farberow, Carrie A.; ...

    2016-01-21

    Ex situ catalytic fast pyrolysis (CFP) is a promising route for producing fungible biofuels; however, this process requires bifunctional catalysts that favor C–O bond cleavage, activate hydrogen at near atmospheric pressure and high temperature (350–500 °C), and are stable under high-steam, low hydrogen-to-carbon environments. Recently, early transition-metal carbides have been reported to selectively cleave C–O bonds of alcohols, aldehydes, and oxygenated aromatics, yet there is limited understanding of the metal carbide surface chemistry under reaction conditions and the identity of the active sites for deoxygenation. In this study, we evaluated molybdenum carbide (Mo2C) for the deoxygenation of acetic acid, anmore » abundant component of biomass pyrolysis vapors, under ex situ CFP conditions, and we probed the Mo2C surface chemistry, identity of the active sites, and deoxygenation pathways using in situ diffuse reflectance infrared Fourier transform spectroscopy (DRIFTS), X-ray photoelectron spectroscopy (XPS), and density functional theory (DFT) calculations.« less

  11. Rheological and hydrodynamic properties of cellulose acetate/ionic liquid solutions.

    PubMed

    Rudaz, Cyrielle; Budtova, Tatiana

    2013-02-15

    Rheological properties of cellulose acetate/1-ethyl-3-methylimidazolium acetate (EMIMAc) solutions are studied using shear dynamic and steady state rheology in a large range of polymer concentrations (from 0.1 to 10 wt.%) and temperatures (from 0 °C to 80 °C). Master plots for storage and loss moduli and for dynamic viscosity were built and shift parameters determined. Cellulose acetate/EMIMAc behaves as a classical polymer solution and obeys Cox-Merz law. Cellulose acetate intrinsic viscosity [η] was determined as a function of temperature and compared with the literature data for cellulose acetates dissolved in other solvents and cellulose dissolved in EMIMAc. Cellulose acetate intrinsic viscosity turned out to be much less temperature sensitive than that of cellulose. Specific viscosity-C[η] master plot was built: the slopes in log-log scale are 1.2 and 3.1 in dilute and semi-dilute regions, respectively. The activation energy as a function of concentration follows a power-law dependence.

  12. Activation of TRPV4 by dietary apigenin antagonizes renal fibrosis in deoxycorticosterone acetate (DOCA)-salt-induced hypertension.

    PubMed

    Wei, Xing; Gao, Peng; Pu, Yunfei; Li, Qiang; Yang, Tao; Zhang, Hexuan; Xiong, Shiqiang; Cui, Yuanting; Li, Li; Ma, Xin; Liu, Daoyan; Zhu, Zhiming

    2017-04-01

    Hypertension-induced renal fibrosis contributes to the progression of chronic kidney disease, and apigenin, an anti-hypertensive flavone that is abundant in celery, acts as an agonist of transient receptor potential vanilloid 4 (TRPV4). However, whether apigenin reduces hypertension-induced renal fibrosis, as well as the underlying mechanism, remains elusive. In the present study, the deoxycorticosterone acetate (DOCA)-salt hypertension model was established in male Sprague-Dawley rats that were treated with apigenin or vehicle for 4 weeks. Apigenin significantly attenuated the DOCA-salt-induced structural and functional damage to the kidney, which was accompanied by reduced expression of transforming growth factor-β1 (TGF-β1)/Smad2/3 signaling pathway and extracellular matrix proteins. Immunochemistry, cell-attached patch clamp and fluorescent Ca(2+) imaging results indicated that TRPV4 was expressed and activated by apigenin in both the kidney and renal cells. Importantly, knockout of TRPV4 in mice abolished the beneficial effects of apigenin that were observed in the DOCA-salt hypertensive rats. Additionally, apigenin directly inhibited activation of the TGF-β1/Smad2/3 signaling pathway in different renal tissues through activation of TRPV4 regardless of the type of pro-fibrotic stimulus. Moreover, the TRPV4-mediated intracellular Ca(2+) influx activated the AMP-activated protein kinase (AMPK)/sirtuin 1 (SIRT1) pathway, which inhibited the TGF-β1/Smad2/3 signaling pathway. In summary, dietary apigenin has beneficial effects on hypertension-induced renal fibrosis through the TRPV4-mediated activation of AMPK/SIRT1 and inhibition of the TGF-β1/Smad2/3 signaling pathway. This work suggests that dietary apigenin may represent a promising lifestyle modification for the prevention of hypertension-induced renal damage in populations that consume a high-sodium diet.

  13. Synthesis and anticarcinogenic activity of 5-fluorouracil-1-acetic acid complexes with rare earths

    SciTech Connect

    Wang Liu-Fang; Yang Zheng-Yin; Peng Zhou-Ren ); Cheng Guo-Quan; Guo Hong-Ying; Sun Al-Li ); Wang QI; He Feng Ying )

    1993-01-01

    Thirteen new solid complexes of 5-fluorouracilacetic acid (FAA) with rare earth metals (RE) have been synthesized. Elemental analysis, IR, UV spectra, TG-DTA, conductance measurements and [sup 1]H NMR spectra have been used to characterise them. The general formula of the complexes is Ln(FAA)[sub 3][center dot]2H[sub 2]O (Ln = La [yields] Yb, Pm not included). The anticarcinogenic activity of La(FAA)[sub 3][center dot]2H[sub 2]O was tested. The results obtained showed that the survival period of mice which had been transplanted with ascites carcinoma (HepA) and then treated with the La complex can be prolonged to 235% of the control but the ligand alone showed little anticarcinogenic activity. Some 42% of EC cancer cell growth can be inhibited by the La complex. the LD[sub 50] is 500 mg kg[sup [minus

  14. Antioxidant and larvicidal activities of Tephrosia egregia Sandw against Aedes aegypti.

    PubMed

    Arriaga, Angela M C; Lima, Jefferson Q; e Vasconcelos, Jackson N; de Oliveira, Maria C F; Lemos, Telma L G; Fonseca, Aluisio M; Malcher, Grazielle T; Santiago, Gilvandete M P; Mafezoli, J; Braz-Filho, Raimundo

    2009-04-01

    The antioxidant and larvicidal activities of Tephrosia egregia extracts and its major component, dehydrorotenone, were studied. High antioxidant activity was found for dehydrorotenone and methanol and ethyl acetate extracts from roots and stems, respectively. Among the tested extracts, the hexane extract from stems showed potent larvicidal activity (LC50 12.88 +/- 0.64) while low activity was found for dehydrorotenone.

  15. Metabolism of (2-14C)acetate and its use in assessing hepatic Krebs cycle activity and gluconeogenesis

    SciTech Connect

    Schumann, W.C.; Magnusson, I.; Chandramouli, V.; Kumaran, K.; Wahren, J.; Landau, B.R. )

    1991-04-15

    To examine the fate of the carbons of acetate and to evaluate the usefulness of labeled acetate in assessing intrahepatic metabolic processes during gluconeogenesis, (2-14C)acetate, (2-14C)ethanol, and (1-14C)ethanol were infused into normal subjects fasted 60 h and given phenyl acetate. Distributions of 14C in the carbons of blood glucose and glutamate from urinary phenylacetylglutamine were determined. With (2-14C)acetate and (2-14C)ethanol, carbon 1 of glucose had about twice as much 14C as carbon 3. Carbon 2 of glutamate had about twice as much 14C as carbon 1 and one-half to one-third as much as carbon 4. There was only a small amount in carbon 5. These distributions are incompatible with the metabolism of (2-14C)acetate being primarily in liver. Therefore, (2-14C)acetate cannot be used to study Krebs cycle metabolism in liver and in relationship to gluconeogenesis, as has been done. The distributions can be explained by: (a) fixation of 14CO2 from (2-14C)acetate in the formation of the 14C-labeled glucose and glutamate in liver and (b) the formation of 14C-labeled glutamate in a second site, proposed to be muscle. (1,3-14C)Acetone formation from the (2-14C)acetate does not contribute to the distributions, as evidenced by the absence of 14C in carbons 2-4 of glutamate after (1-14C)ethanol administration.

  16. Molecular basis of neuroprotective activities of rasagiline and the anti-Alzheimer drug TV3326 [(N-propargyl-(3R)aminoindan-5-YL)-ethyl methyl carbamate].

    PubMed

    Youdim, M B; Weinstock, M

    2001-12-01

    Rasagiline (N-propargyl-1-(R)-aminoindan) is a selective, irreversible monoamine oxidase B (MAO B) inhibitor which has been developed as an anti-Parkinson drug. In controlled monotherapy and as adjunct to L-dopa it has shown anti-Parkinson activity. In cell culture (PC-12 and neuroblastoma SH-SY5Y cells) it exhibits neuroprotective and anti-apoptotic activity against several neurotoxins (SIN-1, MPTP, 6-hydroxydopamine and N-methyl-(R)-salsolinol) and ischemia. In vivo, it reduces the sequelae of traumatic brain injury in mice and speeds their recovery. The neuroprotective activity of rasagaline does not result from MAO B inhibition, since its S-enantiomer, TVP1022, which has 1000-fold weaker MAO inhibitory activity, exhibits similar neuroprotective properties. Introduction of a carbamate moiety into the rasagiline molecule to confer cholinesterase inhibitory activity for the treatment of Alzheimer's disease, resulted in compounds TV3326 [(N-Propargyl-(3R)Aminoindan-5-YL)-Ethyl Methyl Carbamate] and its S-enantiomer TV3279 [(N-Propargyl-(3S)Aminoindan-5-YL)-Ethyl Methyl Carbamate], which retain the neuroprotective activities of rasagiline and TVP1022. They also antagonize scopolamine-induced impairments in spatial memory. In addition, TV3326 exhibits brain-selective MAO A and B inhibitory activity after chronic administration and has antidepressant-like activity in the forced swim test. This is associated with an increase in brain levels of serotonin. The anti-apoptotic activity of these propargylamine-containing derivatives may be related to their ability to delay the opening of voltage-dependent anion channels (VDAC), which are part of the mitochondrial permeability transition pore. The propargylamine moiety is responsible for the increase in the mitochondrial family of Bcl-2 proteins, prevention in the fall in mitochondrial membrane potential, prevention of the activation of caspase 3, and of translocation of glyceraldehyde-3-phosphate dehydrogenase from the

  17. Significant and Sustained Antitumor Activity in Post-Docetaxel, Castration-Resistant Prostate Cancer With the CYP17 Inhibitor Abiraterone Acetate

    PubMed Central

    Reid, Alison H.M.; Attard, Gerhardt; Danila, Daniel C.; Oommen, Nikhil Babu; Olmos, David; Fong, Peter C.; Molife, L. Rhoda; Hunt, Joanne; Messiou, Christina; Parker, Christopher; Dearnaley, David; Swennenhuis, Joost F.; Terstappen, Leon W.M.M.; Lee, Gloria; Kheoh, Thian; Molina, Arturo; Ryan, Charles J.; Small, Eric; Scher, Howard I.; de Bono, Johann S.

    2010-01-01

    Purpose The principal objective of this trial was to evaluate the antitumor activity of abiraterone acetate, an oral, specific, irreversible inhibitor of CYP17 in docetaxel-treated patients with castration-resistant prostate cancer (CRPC). Patients and Methods In this multicenter, two-stage, phase II study, abiraterone acetate 1,000 mg was administered once daily continuously. The primary end point was achievement of a prostate-specific antigen (PSA) decline of ≥ 50% in at least seven of 35 patients. Per an attained phase II design, more than 35 patients could be enrolled if the primary end point was met. Secondary objectives included: PSA declines of ≥ 30% and ≥ 90%; rate of RECIST (Response Evaluation Criteria in Solid Tumors) responses and duration on study; time to PSA progression; safety and tolerability; and circulating tumor cell (CTC) enumeration. Results Docetaxel-treated patients with CRPC (N = 47) were enrolled. PSA declines of ≥ 30%, ≥ 50% and ≥ 90% were seen in 68% (32 of 47), 51% (24 of 47), and 15% (seven of 47) of patients, respectively. Partial responses (by RECIST) were reported in eight (27%) of 30 patients with measurable disease. Median time to PSA progression was 169 days (95% CI, 113 to 281 days). The median number of weeks on study was 24, and 12 (25.5%) of 47 patients remained on study ≥ 48 weeks. CTCs were enumerated in 34 patients; 27 (79%) of 34 patients had at least five CTCs at baseline. Eleven (41%) of 27 patients had a decline from at least five to less than 5 CTCs, and 18 (67%) of 27 had a ≥ 30% decline in CTCs after starting treatment with abiraterone acetate. Abiraterone acetate was well tolerated. Conclusion Abiraterone acetate has significant antitumor activity in post-docetaxel patients with CRPC. Randomized, phase III trials of abiraterone acetate are underway to define the future role of this agent. PMID:20159823

  18. Production of bio-oil rich in acetic acid and phenol from fast pyrolysis of palm residues using a fluidized bed reactor: Influence of activated carbons.

    PubMed

    Jeong, Jae-Yong; Lee, Uen-Do; Chang, Won-Seok; Jeong, Soo-Hwa

    2016-11-01

    In this study, palm residues were pyrolyzed in a bench-scale (3kg/h) fast pyrolysis plant equipped with a fluidized bed reactor and bio-oil separation system for the production of bio-oil rich in acetic acid and phenol. Pyrolysis experiments were performed to investigate the effects of reaction temperature and the types and amounts of activated carbon on the bio-oil composition. The maximum bio-oil yield obtained was approximately 47wt% at a reaction temperature of 515°C. The main compounds produced from the bio-oils were acetic acid, hydroxyacetone, phenol, and phenolic compounds such as cresol, xylenol, and pyrocatechol. When coal-derived activated carbon was applied, the acetic acid and phenol yields in the bio-oils reached 21 and 19wt%, respectively. Finally, bio-oils rich in acetic acid and phenol could be produced separately by using an in situ bio-oil separation system and activated carbon as an additive.

  19. Chlorimuron-ethyl

    Integrated Risk Information System (IRIS)

    Chlorimuron - ethyl ; CASRN 90982 - 32 - 4 Human health assessment information on a chemical substance is included in the IRIS database only after a comprehensive review of toxicity data , as outlined in the IRIS assessment development process . Sections I ( Health Hazard Assessments for Noncarcinog

  20. Methyl ethyl ketone (MEK)

    Integrated Risk Information System (IRIS)

    EPA 635 / R - 03 / 009 www.epa.gov / iris TOXICOLOGICAL REVIEW OF METHYL ETHYL KETONE ( CAS No . 78 - 93 - 3 ) In Support of Summary Information on the Integrated Risk Information System ( IRIS ) September 2003 U.S . Environmental Protection Agency Washington , DC DISCLAIMER This document has been r

  1. Ethyl alcohol production

    SciTech Connect

    Hofman, V.; Hauck, D.

    1980-11-01

    Recent price increases and temporary shortages of petroleum products have caused farmers to search for alternate sources of fuel. The production of ethyl alcohol from grain is described and the processes involved include saccharification, fermentation and distillation. The resulting stillage has potential as a livestock feed.

  2. Design, Synthesis and Anti-Tubercular Activity of Novel 1, 4-Dihydropyrine-3, 5-Dicarboxamide Containing 4(5)-Chloro-2-Ethyl- 5(4)-Imidazolyl Moiety

    PubMed Central

    Iman, Maryam; Davood, Asghar; Lotfinia, Mahboubeh; Dehqani, Golnoush; Sardari, Soroush; Azerang, Parisa; Amini, Mohsen

    2016-01-01

    Current researches have showed that N3, N5-diaryl-2, 6-dimethyl -1, 4-dihydropyrine-3, 5- dicarboxamide analogues demonstrate notable anti-tubercular activity. In this study, Hantzsch condensation was used to design and synthesize new analogues of dihydropyridine (DHP). Different diary carboxamides were inserted at positions 3 and 5 of the DHP ring. 4(5)-chloro-2-ethyl-5(4)-imidazolyl moiety was considered at position 4 of the DHP ring. The structures of prepared ligands were characterized using TLC followed by FT-IR, elemental analysis, Mass and proton NMR. Results of anti-tubercular activity have indicated all the prepared ligands 3a-f inhibit the mycobacterium tuberculosis growth and the most potent compounds were 3c (3,4-Cl) and 3b (4-Cl). The in-vitro obtained data are agreement with our computational predictions in terms of partial atomic charge of carbonyl moieties at the positions 3 and 5 of dihydropyridine ring and the logP of the molecules. PMID:28243275

  3. Screening of solvent dependent antibacterial activity of Prunus domestica.

    PubMed

    Yaqeen, Zahra; Naqvi, Naim-ul-Hasan; Sohail, Tehmina; Rehman, Zakir-ur; Fatima, Nudrat; Imran, Hina; Rehman, Atiqur

    2013-03-01

    Fruit of Prunus domestica was extracted in ethanol. The ethanol extract was further extracted with two solvents ethyl acetate and chloroform. The crude ethanol extract and two fractions (ethyl acetate and chloroform) were screened for their antibacterial activity using the agar well diffusion method .They were tested against nine bacteria; five Gram positive bacteria (Staphylococcus aureus, Streptococcuc intermedius, Bacillus cereus, Bacillus pumilus) and four Gram negative bacteria (Eschrichia coli, Proteus mirabilis Shigella flexneri, Salmonella typhi and Klebsiela pneumoniae). The susceptibility of microorganisms to all three fractions was compared with each other and with standard antibiotic (Ampicillin) Among all fractions ethyl acetate exhibited highest antibacterial activity (average zone of inhibition 34.57mm ± 1.3) while ethyl alcohol exhibited least antibacterial activity (average zone of inhibition 17.42mm ± 3.3). Minimum inhibitory concentration of ethanol, ethyl acetate and chloroform fractions was found in the range of 78 μ g/ml to 2500 μ gl/ml against gram positive and gram negative bacteria.

  4. Biosorption of formic and acetic acids from aqueous solution using activated carbon from shea butter seed shells

    NASA Astrophysics Data System (ADS)

    Adekola, Folahan A.; Oba, Ismaila A.

    2016-10-01

    The efficiency of prepared activated carbon from shea butter seed shells (SB-AC) for the adsorption of formic acid (FA) and acetic acid (AA) from aqueous solution was investigated. The effect of optimization parameters including initial concentration, agitation time, adsorbent dosage and temperature of adsorbate solution on the sorption capacity were studied. The SB-AC was characterized for the following parameters: bulk density, moisture content, ash content, pH, Fourier transform infrared spectroscopy (FTIR) and scanning electron microscopy (SEM). The optimal conditions for the adsorption were established and the adsorption data for AA fitted Dubinin-Radushkevich (D-R) isotherm well, whereas FA followed Langmuir isotherm. The kinetic data were examined. It was found that pseudo-second-order kinetic model was found to adequately explain the sorption kinetic of AA and FA from aqueous solution. It was again found that intraparticle diffusion was found to explain the adsorption mechanism. Adsorption thermodynamic parameters were estimated and the negative values of ∆G showed that the adsorption process was feasible and spontaneous in nature, while the negative values of ∆H indicate that the adsorption process was exothermic. It is therefore established that SB-AC has good potential for the removal of AA and FA from aqueous solution. Hence, it should find application in the regular treatment of polluted water in aquaculture and fish breeding system.

  5. Intra- and intermolecular alkylation of N,O-acetals and π-activated alcohols catalyzed by in situ generated acid.

    PubMed

    Hamon, Mélanie; Dickinson, Niall; Devineau, Alice; Bolien, David; Tranchant, Marie-José; Taillier, Catherine; Jabin, Ivan; Harrowven, David C; Whitby, Richard J; Ganesan, A; Dalla, Vincent

    2014-03-07

    Intramolecular and intermolecular alkylations of carbocation precursors of limited ionization ability, principally N,O-acetals, without the use of an exogenous reagent have been developed. The reactions are carried out in 1,1,2,2-tetrachloroethane (TCE) and take advantage of the ability of this solvent to continuously release small amounts of HCl by thermolytic elimination. A study of the reaction led to several improved protocols such as (1) preheated TCE, (2) microwave-assisted reactions, and (3) flow or sealed-tube conditions, which allow significant reaction rate enhancements and made possible some challenging reactions such as the α-amidoalkylation of ketones. Studies using flow chemistry confirmed not only that very low concentrations of HCl generated from the solvent were responsible for the reactivity but also that TCE had additional beneficial properties in comparison to other chlorinated solvents such as dichloroethane. The method can easily be extended to the alkylation using proelectrophiles such as π-activated alcohols, which are normally unreactive toward HCl catalysis. This work represents the first successful use of HCl, the simplest strong Brønsted acid, as an efficient alkylation catalyst.

  6. Effect of gossypol-acetic acid on calcium transport and ATPase activity in plasma membranes from ram and bull spermatozoa.

    PubMed

    Breitbart, H; Rubinstein, S; Nass-Arden, L

    1984-10-01

    The effects of gossypol acetic acid on the activity of Mg-ATPase and Ca-Mg-ATPase and on calcium uptake by plasma membranes from ram and bull spermatozoa were examined. The three parameters were almost completely inhibited by 10 microM gossypol for both ram and bull sperm. In order to assess the effects of higher gossypol concentrations isolated membrane vesicles were loaded with calcium by operating the ATP-dependent calcium pump after which gossypol was added and calcium uptake followed. At 10 microM gossypol, additional calcium uptake was 85% inhibited while at 40 microM a release of the accumulated calcium was observed. The inhibitory effect of 10 microM gossypol was almost completely reversible by simple dilution of gossypol-treated membranes, whilst at 40 microM the effect was only 50% reversible. The data show a high degree of similarity between bull and ram, suggesting minimal differences between the two species as far as the structure and function of the sperm plasma membrane is concerned.

  7. Diclofenac sodium loaded-cellulose acetate butyrate: effect of processing variables on microparticles properties, drug release kinetics and ulcerogenic activity.

    PubMed

    Barakat, Nahla S; Ahmad, Amany A E

    2008-02-01

    The aim of this study was to develop and characterize diclofenac sodium loaded-cellulose acetate butyrate microparticles in order to obtain a controlled-release system. The influence of the type of polymer, the volume and composition of the internal phase, drug loading, surfactant concentration and additive added on microparticles characteristics (particle size, encapsulation efficiency, surface morphology and in vitro release profiles) was studied to optimize the microparticles system. The resultant microparticles were evaluated for the recovery, average particle size, drug loading and incorporation efficiency. The microparticles exhibited good flowing nature and compressibility index when compared to pure drug. Dissolution rate of diclofenac sodium in phosphate buffer (pH 6.8) increased with increases in initial drug loading, surfactant concentration and addition of alcohol as co-solvent but decreased with increases in the concentration of additives such as Gantrez AN or Eudragit S100 in the internal phase. The dissolution data showed a Higuchi diffusion pattern for most of the formulations. About 56-81% reduction in ulcerogenic activity was observed with microparticles containing Eudragit S100 17-25%, based on total polymer concentration, when compared with pure diclofenac sodium.

  8. Active-Site Engineering of ω-Transaminase for Production of Unnatural Amino Acids Carrying a Side Chain Bulkier than an Ethyl Substituent

    PubMed Central

    Han, Sang-Woo; Park, Eul-Soo; Dong, Joo-Young

    2015-01-01

    ω-Transaminase (ω-TA) is a promising enzyme for use in the production of unnatural amino acids from keto acids using cheap amino donors such as isopropylamine. The small substrate-binding pocket of most ω-TAs permits entry of substituents no larger than an ethyl group, which presents a significant challenge to the preparation of structurally diverse unnatural amino acids. Here we report on the engineering of an (S)-selective ω-TA from Ochrobactrum anthropi (OATA) to reduce the steric constraint and thereby allow the small pocket to readily accept bulky substituents. On the basis of a docking model in which l-alanine was used as a ligand, nine active-site residues were selected for alanine scanning mutagenesis. Among the resulting variants, an L57A variant showed dramatic activity improvements in activity for α-keto acids and α-amino acids carrying substituents whose bulk is up to that of an n-butyl substituent (e.g., 48- and 56-fold increases in activity for 2-oxopentanoic acid and l-norvaline, respectively). An L57G mutation also relieved the steric constraint but did so much less than the L57A mutation did. In contrast, an L57V substitution failed to induce the improvements in activity for bulky substrates. Molecular modeling suggested that the alanine substitution of L57, located in a large pocket, induces an altered binding orientation of an α-carboxyl group and thereby provides more room to the small pocket. The synthetic utility of the L57A variant was demonstrated by carrying out the production of optically pure l- and d-norvaline (i.e., enantiomeric excess [ee] > 99%) by asymmetric amination of 2-oxopantanoic acid and kinetic resolution of racemic norvaline, respectively. PMID:26231640

  9. Insights on the Phytochemical Profile (Cyclopeptides) and Biological Activities of Calotropis procera Latex Organic Fractions

    PubMed Central

    Jucá, Thiago Lustosa; Ramos, Márcio Viana; Moreno, Frederico Bruno Mendes Batista; Viana de Matos, Mayara Patrícia; Marinho-Filho, José Delano Barreto; Moreira, Renato Azevedo; Monteiro-Moreira, Ana Cristina de Oliveira

    2013-01-01

    Calotropis procera is a medicinal plant whose pharmacological properties are associated with its latex. Here, the Calotropis procera latex fractions were investigated in an attempt to trace its phytochemical profile and measure its anti-inflammatory and toxicity activity. The crude latex was partitioned, yielding five fractions (49.4% hexane, 5.2% dichloromethane, 2.0% ethyl acetate, 2.1% n-butanol, and 41.1% aqueous). Phytochemical screening and spectroscopy analysis revealed that dichloromethane is the most chemically diverse fraction. Triterpenes were detected in both the hexane and dichloromethane fractions, while flavonoids were detected in the dichloromethane and ethyl acetate fractions. These fractions were cytotoxic to cancer cell lines (LD50 0.05 to 3.9 μg/mL) and lethal to brine shrimp (LD50 10.9 to 65.7 μg/mL). Reduced neutrophil migration in rats was observed in carrageenan-induced peritonitis for the dichloromethane (67%), ethyl acetate (56%), and aqueous (72%) fractions. A positive reaction with tolidine and ninhydrin suggested that cyclopeptides are in the ethyl acetate fraction. It is therefore concluded that Calotropis procera latex dichloromethane and ethyl acetate fractions exhibit both in vitro and in vivo activities as well as anti-inflammatory properties. Cyclopeptide detection is especially interesting because previous attempts to investigate these low-molecular cyclic amino acid sequences in C. procera have failed. PMID:24348174

  10. The Arabidopsis transcription factor BRASSINOSTEROID INSENSITIVE1-ETHYL METHANESULFONATE-SUPPRESSOR1 is a direct substrate of MITOGEN-ACTIVATED PROTEIN KINASE6 and regulates immunity.

    PubMed

    Kang, Sining; Yang, Fan; Li, Lin; Chen, Huamin; Chen, She; Zhang, Jie

    2015-03-01

    Pathogen-associated molecular patterns (PAMPs) are recognized by plant pattern recognition receptors to activate PAMP-triggered immunity (PTI). Mitogen-activated protein kinases (MAPKs), as well as other cytoplasmic kinases, integrate upstream immune signals and, in turn, dissect PTI signaling via different substrates to regulate defense responses. However, only a few direct substrates of these signaling kinases have been identified. Here, we show that PAMP perception enhances phosphorylation of BRASSINOSTEROID INSENSITIVE1-ETHYL METHANESULFONATE-SUPPRESSOR1 (BES1), a transcription factor involved in brassinosteroid (BR) signaling pathway, through pathogen-induced MAPKs in Arabidopsis (Arabidopsis thaliana). BES1 interacts with MITOGEN-ACTIVATED PROTEIN KINASE6 (MPK6) and is phosphorylated by MPK6. bes1 loss-of-function mutants display compromised resistance to bacterial pathogen Pseudomonas syringae pv tomato DC3000. BES1 S286A/S137A double mutation (BES1(SSAA)) impairs PAMP-induced phosphorylation and fails to restore bacterial resistance in bes1 mutant, indicating a positive role of BES1 phosphorylation in plant immunity. BES1 is phosphorylated by glycogen synthase kinase3 (GSK3)-like kinase BR-insensitive2 (BIN2), a negative regulator of BR signaling. BR perception inhibits BIN2 activity, allowing dephosphorylation of BES1 to regulate plant development. However, BES1(SSAA) does not affect BR-mediated plant growth, suggesting differential residue requirements for the modulation of BES1 phosphorylation in PTI and BR signaling. Our study identifies BES1 as a unique direct substrate of MPK6 in PTI signaling. This finding reveals MAPK-mediated BES1 phosphorylation as another BES1 modulation mechanism in plant cell signaling, in addition to GSK3-like kinase-mediated BES1 phosphorylation and F box protein-mediated BES1 degradation.

  11. High power density supercapacitors based on the carbon dioxide activated D-glucose derived carbon electrodes and 1-ethyl-3-methylimidazolium tetrafluoroborate ionic liquid

    NASA Astrophysics Data System (ADS)

    Tooming, T.; Thomberg, T.; Kurig, H.; Jänes, A.; Lust, E.

    2015-04-01

    The electrochemical impedance spectroscopy, cyclic voltammetry, constant current charge/discharge and the constant power discharge methods have been applied to establish the electrochemical characteristics of the electrical double-layer capacitor (EDLC) consisting of the 1-ethyl-3-methylimidazolium tetrafluoroborate (EMImBF4) ionic liquid and microporous carbon electrodes. Microporous carbon material used for preparation of electrodes (GDAC - glucose derived activated carbon), has been synthesised from D-(+)-glucose by the hydrothermal carbonization method, including subsequent pyrolysis, carbon dioxide activation and surface cleaning step with hydrogen. The Brunauer-Emmett-Teller specific surface area (SBET = 1540 m2 g-1), specific surface area calculated using the non-local density functional theory in conjunction with stable adsorption integral equation using splines (SAIEUS) model SSAIEUS = 1820 m2 g-1, micropore surface area (Smicro = 1535 m2 g-1), total pore volume (Vtot = 0.695 cm3 g-1) and the pore size distribution were obtained from the N2 sorption data. The SBET, Smicro and Vtot values have been correlated with the electrochemical characteristics strongly dependent on the carbon activation conditions applied for EDLCs. Wide region of ideal polarizability (ΔV ≤ 3.2 V), very short charging/discharging time constant (2.7 s), and high specific series capacitance (158 F g-1) have been calculated for the optimized carbon material GDAC-10h (activation of GDAC with CO2 during 10 h) in EMImBF4 demonstrating that this system can be used for completing the EDLC with high energy- and power densities.

  12. Antifungal activity of Cynara scolymus L. extracts.

    PubMed

    Zhu, X F; Zhang, H X; Lo, R

    2005-01-01

    Chloroform, ethanol and ethyl acetate extracts of Cynara scolymus L. leaves, heads and stems were tested for their antifungal activity using the agar-well diffusion assay technique. The leaves extracts and the ethanol fractions were found to be the most effective extract against all the tested organisms.

  13. Trypanocidal activity of the ethyl esters of N-propyl and N-isopropyl oxamates on intracellular amastigotes of Trypanosoma cruzi acute infected mice.

    PubMed

    Aguirre-Alvarado, Charmina; Zaragoza-Martínez, Fabiola; Rodríguez-Páez, Lorena; Téllez-Rendón, Juan Luis; Nogueda, Benjamín; Baeza, Isabel; Wong, Carlos

    2010-02-01

    In this investigation we studied the trypanocidal activity of the ethyl esters of N-propyl (Et-NPOX) and N-isopropyl (Et-NIPOX) oxamates on bloodstream trypomastigotes and on the clinically relevant intracellular amastigotes of Trypanosoma cruzi acute infected mice. In the infected and treated mice, the levels of parasitemia were drastically reduced between days 15 and 20 of treatment and almost to zero between days 35 and 40. We also found that Et-NPOX completely eliminated amastigote nests in the myocardium of mice infected with INC-5 or NINOA T. cruzi strain, and in skeletal muscle the reduction in the number of amastigote nests was between 60 and 80% in both strains. Also, Et-NIPOX reduced by 60-80% the number of amastigote nests in the myocardium and skeletal muscle of mice infected with these T. cruzi strains. In contrast, nifurtimox, used for comparison, produced a reduction of amastigote nests of only 20-40% in the studied tissues in both strains.

  14. Quantitation using a stable isotope dilution assay (SIDA) and thresholds of taste-active pyroglutamyl decapeptide ethyl esters (PGDPEs) in sake.

    PubMed

    Hashizume, Katsumi; Ito, Toshiko; Igarashi, Shinya

    2017-03-01

    A stable isotope dilution assay (SIDA) for two taste-active pyroglutamyl decapeptide ethyl esters (PGDPE1; (pGlu)LFGPNVNPWCOOC2H5, PGDPE2; (pGlu)LFNPSTNPWCOOC2H5) in sake was developed using deuterated isotopes and high-resolution mass spectrometry. Recognition thresholds of PGDPEs in sake were estimated as 3.8 μg/L for PGDPE1 and 8.1 μg/L for PGDPE2, evaluated using 11 student panelists aged in their twenties. Quantitated concentrations in 18 commercial sake samples ranged from 0 to 27 μg/L for PGDPE1 and from 0 to 202 μg/L for PGDPE2. The maximum levels of PGDPE1 and PGDPE2 in the sake samples were approximately 8 and 25 times higher than the estimated recognition thresholds, respectively. The results indicated that PGDPEs may play significant sensory roles in the sake. The level of PGDPEs in unpasteurized sake samples decreased during storage for 50 days at 6 °C, suggesting PGDPEs may be enzymatically decomposed.

  15. GC-MS and GC-MS/MS measurement of ibuprofen in 10-μL aliquots of human plasma and mice serum using [α-methylo-(2)H3]ibuprofen after ethyl acetate extraction and pentafluorobenzyl bromide derivatization: Discovery of a collision energy-dependent H/D isotope effect and pharmacokinetic application to inhaled ibuprofen-arginine in mice.

    PubMed

    Tsikas, Dimitrios; Kayacelebi, Arslan Arinc; Hanff, Erik; Mitschke, Anja; Beckmann, Bibiana; Tillmann, Hanns-Christian; Gutzki, Frank-Mathias; Müller, Meike; Bernasconi, Corrado

    2017-02-01

    GC-MS and GC-MS/MS methods were developed and validated for the quantitative determination of ibuprofen (d0-ibuprofen), a non-steroidal anti-inflammatory drug (NSAID), in human plasma using α-methyl-(2)H3-4-(isobutyl)phenylacetic acid (d3-ibuprofen) as internal standard. Plasma (10μL) was diluted with acetate buffer (80μL, 1M, pH 4.9) and d0- and d3-ibuprofen were extracted with ethyl acetate (2×500μL). After solvent evaporation d0- and d3-ibuprofen were derivatized in anhydrous acetonitrile by using pentafluorobenzyl (PFB) bromide and N,N-diisopropylethylamine as the base catalyst. Under electron-capture negative-ion chemical ionization (ECNICI), the PFB esters of d0- and d3-ibuprofen readily ionize to form their carboxylate anions [M-PFB](-) at m/z 205 and m/z 208, respectively. Collision-induced dissociation (CID) of m/z 205 and m/z 208 resulted in the formation of the anions at m/z 161 and m/z 164, respectively, due to neutral loss of CO2 (44 Da). A collision energy-dependent H/D isotope effect was observed, which involves abstraction/elimination of H(-) from d0-ibuprofen and D(-) from d3-ibuprofen and is minimum at a CE value of 5eV. Quantitative GC-MS determination was performed by selected-ion monitoring of m/z 205 and m/z 208. Quantitative GC-MS/MS determination was performed by selected-reaction monitoring of the mass transitions m/z 205 to m/z 161 for d0-ibuprofen and m/z 208 to m/z 164 for d3-ibuprofen. In a therapeutically relevant concentration range (0-1000μM) d0-ibuprofen added to human plasma was determined with accuracy (recovery, %) and imprecision (relative standard deviation, %) ranging between 93.7 and 110%, and between 0.8 and 4.9%, respectively. GC-MS (y) and GC-MS/MS (x) yielded almost identical results (y=4.00+0.988x, r(2)=0.9991). In incubation mixtures of arachidonic acid (10μM), d3-ibuprofen (10μM) or d0-ibuprofen (10μM) with ovine cyclooxygenase (COX) isoforms 1 and 2, the concentration of d3-ibuprofen and d0-ibuprofen did not

  16. Alteration of seed fatty acid composition by an ethyl methanesulfonate-induced mutation in Arabidopsis thaliana affecting diacylglycerol acyltransferase activity.

    PubMed Central

    Katavic, V; Reed, D W; Taylor, D C; Giblin, E M; Barton, D L; Zou, J; Mackenzie, S L; Covello, P S; Kunst, L

    1995-01-01

    In characterizing the enzymes involved in the formation of very long-chain fatty acids (VLCFAs) in the Brassicaceae, we have generated a series of mutants of Arabidopsis thaliana that have reduced VLCFA content. Here we report the characterization of a seed lipid mutant, AS11, which, in comparison to wild type (WT), has reduced levels of 20:1 and 18:1 and accumulates 18:3 as the major fatty acid in triacylglycerols. Proportions of 18:2 remain similar to WT. Genetic analyses indicate that the fatty acid phenotype is caused by a semidominant mutation in a single nuclear gene, designated TAG1, located on chromosome 2. Biochemical analyses have shown that the AS11 phenotype is not due to a deficiency in the capacity to elongate 18:1 or to an increase in the relative delta 15 or delta 12 desaturase activities. Indeed, the ratio of desaturase/elongase activities measured in vitro is virtually identical in developing WT and AS11 seed homogenates. Rather, the fatty acid phenotype of AS11 is the result of reduced diacylglycerol acyltransferase activity throughout development, such that triacylglycerol biosynthesis is reduced. This leads to a reduction in 20:1 biosynthesis during seed development, leaving more 18:1 available for desaturation. Thus, we have demonstrated that changes to triacylglycerol biosynthesis can result in dramatic changes in fatty acid composition and, in particular, in the accumulation of VLCFAs in seed storage lipids. PMID:7784510

  17. Ethyl N-phenyloxamate.

    PubMed

    García-Báez E, Efrén V; Gómez-Castro, Carlos Z; Höpfl, Herbert; Martínez-Martínez, Francisco J; Padilla-Martínez, Itzia I

    2003-10-01

    The oxamate group in the title compound, C(10)H(11)NO(3), is almost coplanar with the phenyl ring because of intramolecular hydrogen-bonding interactions, and the structure can be described as an anilide single bonded to an ethyl carboxylate group. The supramolecular structure is achieved through intermolecular hard N-H...O and soft C-H...X (X = O and phenyl) hydrogen-bonding interactions.

  18. The catabolite gene activator protein (CAP) is not required for indole-3-acetic acid to activate transcription of the araBAD operon of Escherichia coli K-12.

    PubMed

    Ebright, R H; Beckwith, J

    1985-01-01

    Kline et al. (1980) have reported that indole-3-acetic acid (IAA) and four other indole derivatives are able to substitute for cAMP in activating expression of the ara regulon of E. coli. We have examined this phenomenon in detail, utilizing fusions between the structural gene for beta-galactosidase and the promoters for the araBAD, araE, and araFG operons. We confirm that IAA potently stimulates transcription from the araBAD promoter. The effect is highly specific to araBAD, as IAA has no, or only slight, effects on the araE and araFG operons. However, contrary to the results of Kline et al., we find that the action of IAA does not require CAP. Thus, IAA fully stimulates the transcription of araBAD in a strain which bears a complete deletion of the crp gene.

  19. N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-(2-nitrophenyl) cyclohexanecarboxamide: a novel pre- and postsynaptic 5-hydroxytryptamine(1A) receptor antagonist active on the lower urinary tract.

    PubMed

    Leonardi, A; Guarneri, L; Poggesi, E; Angelico, P; Velasco, C; Cilia, A; Testa, R

    2001-12-01

    N-[2-[4-(2-Methoxyphenyl)-1-piperazinyl]ethyl]-N-(2-nitrophenyl) cyclohexanecarboxamide (Rec 15/3079) was synthesized with the aim of obtaining a novel compound with 5-hydroxytryptamine (5-HT)(1A) antagonistic properties and activity in controlling bladder function at the level of the central nervous system. Rec 15/3079 showed a selective high affinity for the 5-HT(1A) receptor (K(i) = 0.2 nM). At the human recombinant 5-HT(1A) receptor, Rec 15/3079 acted as a competitive, neutral antagonist in that it did not modify basal [(35)S]guanosine-5'-O-(3-thio)triphosphate binding to HeLa cell membranes but shifted the activation isotherm to 5-HT to the right, in a parallel manner, with a pK(b) value of 10.5. Accordingly, Rec 15/3079 (i.v.) potently antagonized 8-hydroxy-2-dipropylaminotetralin (8-OH-DPAT)-induced hypothermia in mice (ID(50) = 20 microg/kg) and 8-OH-DPAT-induced forepaw treading in rats (ID(50) = 36 microg/kg). In vitro Rec 15/3079 was poorly active in antagonizing carbachol-induced bladder (pD'(2) = 5.03) and norepinephrine-induced urethral (apparent pK(b) = 6) contractions. However, in anesthetized rats, Rec 15/3079 (10-100 microg/kg i.v.) blocked isovolumic bladder contractions with no effect on their amplitude. In conscious rats and guinea pigs with bladders filled with saline, Rec 15/3079 (300-1000 microg/kg i.v.) increased bladder volume capacity (BVC) without affecting bladder contractility. In conscious rats with bladders filled with dilute acetic acid, Rec 15/3079 (300 microg/kg i.v.) reversed the decrease of BVC induced by the acid. To evaluate apparent selective effect on lower urinary tract reflexes, Rec 15/3079 was tested in experimental models for sedative, analgesic, anxiolytic, and antidepressant activity. Rec 15/3079 showed only a slight decrease in the duration of immobility in the behavioral despair test (antidepressant activity) at 1 mg/kg i.v. No anxiolytic activity was observed at 10 mg/kg i.v. No effect was observed in the hot plate

  20. Protective Role for Tissue Inhibitor of Metalloproteinase-4, a Novel Peroxisome Proliferator-Activated Receptor-γ Target Gene, in Smooth Muscle in Deoxycorticosterone Acetate-Salt Hypertension.

    PubMed

    Ketsawatsomkron, Pimonrat; Keen, Henry L; Davis, Deborah R; Lu, Ko-Ting; Stump, Madeliene; De Silva, T Michael; Hilzendeger, Aline M; Grobe, Justin L; Faraci, Frank M; Sigmund, Curt D

    2016-01-01

    Loss of peroxisome proliferator-activated receptor-γ (PPARγ) function causes hypertension, whereas its activation lowers blood pressure. Evidence suggests that these effects may be attributable to PPARγ activity in the vasculature. However, the specific transcriptional targets of PPARγ in vessels remain largely unidentified. In this study, we examined the role of smooth muscle PPARγ during salt-sensitive hypertension and investigated its transcriptional targets and functional effect. Transgenic mice expressing dominant-negative PPARγ (S-P467L) in smooth muscle cells were more prone to deoxycorticosterone acetate-salt-induced hypertension and mesenteric arterial dysfunction compared with nontransgenic controls. Despite similar morphometry at baseline, vascular remodeling in conduit and small arteries was enhanced in S-P467L after deoxycorticosterone acetate-salt treatment. Gene expression profiling in aorta and mesenteric arteries revealed significantly decreased expression of tissue inhibitor of metalloproteinase-4 (TIMP-4) in S-P467L. Expression of TIMP-4 was increased by deoxycorticosterone acetate-salt treatment, but this increase was ablated in S-P467L. Interference with PPARγ activity either by treatment with a PPARγ inhibitor, GW9662, or by expressing P467L PPARγ markedly suppressed TIMP-4 in primary smooth muscle cells. PPARγ binds to a PPAR response element (PPRE) in chromatin close to the TIMP-4 gene in smooth muscle cells, suggesting that TIMP-4 is a novel target of PPARγ. The interference with PPARγ and decrease in TIMP-4 were accompanied by an increase in total matrix metalloproteinase activity. PPARγ-mediated loss of TIMP-4 increased, whereas overexpression of TIMP-4 decreased smooth muscle cell migration in a scratch assay. Our findings highlight a protective mechanism induced by PPARγ in deoxycorticosterone acetate-salt treatment, establishing a novel mechanistic link between PPARγ and TIMP-4.

  1. Effect of chloroquine phosphate and toxic concentrations of lead acetate on Ca2+-ATPase activity in isolates and clones of Plasmodium falciparum.

    PubMed

    Bolaji, O M; Happi, T C; Oduola, A M J; Babafunmi, E A

    2011-12-20

    The basal activity of Ca2+-ATPase in two isolates (NL56, UNC) and two clones (D6, W2) of P.falciparum was assessed. The effects of various concentrations of chloroquine phosphate and toxic concentrations of lead acetate were also evaluated in the clones and strains of P.falciparum. The Ca2+-ATPase activity was measured by monitoring the rate of release of inorganic phosphate from the gamma-position of ATP on spectrophotometer at 820nm wavelength. The various concentrations of chloroquine (3, 6, 9, 12, 18µg/ml) and lead acetate (5, 10, 20, 30, 40µg/ml) on Ca2+-ATPase activity were measured respectively. Chloroquine phosphate inhibited Ca2+-ATPase activity in both the isolates and the cloned strains of P.falciparum in concentration dependent manner. Median Inhibitory concentration of chloroquine (MIC50) estimated from the plot of activity against chloroquine concentration was found to be 2.6mg/ml at pH 7.4 for both the isolates and cloned strains examined. Lead acetate at concentrations 5-20µg/ml inhibited Ca2+-ATPase activity in concentration dependent manner in clone W2 (Chloroquine resistant strain) while the same range of concentrations of lead acetate stimulated the activity of the enzyme in clone D6 (Chloroquine sensitive strain).The inhibitory effect of lead acetate on the enzyme in clone D6 was observed at concentrations above 20µg/ml. The result also suggests that lead ions could modulate and moderate calcium ion homeostasis in P. falciparum via its effect on Ca2+-ATPase activity. Also sufficient influx of lead ions into P. falciparum may transform the biochemical or bioenergetics nature of chloroquine sensitive strain of P. falciparum (D6) to that similar to chloroquine resistant strain (W2). In conclusion, inhibition of Ca2+-ATPase activity of P.falciparum may be part of the mechanism of action of chloroquine in its use as chemotherapy for malaria. The study implies that populations simultaneously exposed to lead pollution and malaria infection may

  2. Theoretical aspects of methyl acetate and methanol activation on MgO(100) and (501) catalyst surfaces with application in FAME production

    NASA Astrophysics Data System (ADS)

    Man, Isabela-Costinela; Soriga, Stefan Gabriel; Parvulescu, Vasile

    2017-01-01

    Density functional theory (DFT) calculations were carried out to study the activation of methyl acetate and methanol on MgO(100) and MgO(501) surfaces and integrated in the context of transesterification, interesterification and glycerolysis reactions used in biodiesel industry. First results indicate the importance of including of dispersion forces in the calculations. On MgO(100) the reverse reactions steps of Csbnd O and Csbnd H dissociations and on MgO(501) the same reverse reaction step of Csbnd H dissociations of methyl acetate are energetically favorable, while the dissociation of Csbnd O bond into methoxide and acetate fragments on the edge of MgO(501) was found to be exothermic with a low activation energy. For methanol, the dissociation of Osbnd H bond on MgO(100) surface in the presence of the second coadsorbed methanol molecule becomes more energetically favoured compared to the isolated molecule, due to the fact that the methoxide fragment is stabilized by intermolecular hydrogen bonding. This is reflected by the decrease of the activation energy of the forward reaction step and the increase of the activation energy of the backward reaction step, increasing the probability to have dissociated molecules among the undissociated ones. These results represent a step forward for better understanding from atomistic point of view the paths of these reactions on these surfaces for the corresponding catalytic processes.

  3. Assessment of the reproductive toxicity of inhalation exposure to ethyl tertiary butyl ether in male mice with normal, low active and inactive ALDH2.

    PubMed

    Weng, Zuquan; Ohtani, Katsumi; Suda, Megumi; Yanagiba, Yukie; Kawamoto, Toshihiro; Nakajima, Tamie; Wang, Rui-Sheng

    2014-04-01

    No data are available regarding aldehyde dehydrogenase 2 (ALDH2) polymorphisms related to the reproductive toxicity possibly caused by ethyl tertiary butyl ether (ETBE). In this study, two inhalation experiments were performed in Aldh2 knockout (KO), heterogeneous (HT) and wild type (WT) C57BL/6 male mice exposed to ETBE, and the data about general toxicity, testicular histopathology, sperm head numbers, sperm motility and sperm DNA damage were collected. The results showed that the 13-week exposure to 0, 500, 1,750 and 5,000 ppm ETBE significantly decreased sperm motility and increased levels of sperm DNA strand breaks and 8-hydroxy-deoxyguanosine in both WT and KO mice, the effects were found in 1,750 and 5,000 ppm groups of WT mice, and all of the three exposed groups of KO mice compared to the corresponding control; furthermore, ETBE also caused decrease in the relative weights of testes and epididymides, the slight atrophy of seminiferous tubules of testis and reduction in sperm numbers of KO mice exposed to ≥500 ppm. In the experiment of exposure to lower concentrations of ETBE (0, 50, 200 and 500 ppm) for 9 weeks, the remarkable effects of ETBE on sperm head numbers, sperm motility and sperm DNA damage were further observed in KO and HT mice exposed to 200 ppm ETBE, but not in WT mice. Our findings suggested that only exposure to high concentrations of ETBE might result in reproductive toxicity in mice with normal active ALDH2, while low active and inactive ALDH2 enzyme significantly enhanced the ETBE-induced reproductive toxicity in mice, even exposed to low concentrations of ETBE, mainly due to the accumulation of acetaldehyde as a primary metabolite of ETBE.

  4. Anaerobic glyoxylate cycle activity during simultaneous utilization of glycogen and acetate in uncultured Accumulibacter enriched in enhanced biological phosphorus removal communities.

    PubMed

    Burow, Luke C; Mabbett, Amanda N; Blackall, Linda L

    2008-10-01

    Enhanced biological phosphorus removal (EBPR) communities protect waterways from nutrient pollution and enrich microorganisms capable of assimilating acetate as polyhydroxyalkanoate (PHA) under anaerobic conditions. Accumulibacter, an important uncultured polyphosphate-accumulating organism (PAO) enriched in EBPR, was investigated to determine the central metabolic pathways responsible for producing PHA. Acetate uptake and assimilation to PHA in Accumulibacter was confirmed using fluorescence in situ hybridization (FISH)-microautoradiography and post-FISH chemical staining. Assays performed with enrichments of Accumulibacter using an inhibitor of glyceraldehyde-3-phosphate dehydrogenase inferred anaerobic glycolysis activity. Significant decrease in anaerobic acetate uptake and PHA production rates were observed using inhibitors targeting enzymes within the glyoxylate cycle. Bioinformatic analysis confirmed the presence of genes unique to the glyoxylate cycle (isocitrate lyase and malate synthase) and gene expression analysis of isocitrate lyase demonstrated that the glyoxylate cycle is likely involved in PHA production. Reduced anaerobic acetate uptake and PHA production was observed after inhibition of succinate dehydrogenase and upregulation of a succinate dehydrogenase gene suggested anaerobic activity. Cytochrome b/b(6) activity inferred that succinate dehydrogenase activity in the absence of external electron acceptors may be facilitated by a novel cytochrome b/b(6) fusion protein complex that pushes electrons uphill to more electronegative electron carriers. Identification of phosphoenolpyruvate carboxylase and phosphoenolpyruvate carboxykinase genes in Accumulibacter demonstrated the potential for interconversion of C(3) intermediates of glycolysis and C(4) intermediates of the glyoxylate cycle. Our findings along with previous hypotheses from analysis of microbiome data and metabolic models for PAOs were used to develop a model for anaerobic carbon

  5. In vitro antimalarial activity of medicinal plant extracts against Plasmodium falciparum.

    PubMed

    Bagavan, Asokan; Rahuman, Abdul Abdul; Kaushik, Naveen Kumar; Sahal, Dinkar

    2011-01-01

    Malaria is a major global public health problem, and the alarming spread of drug resistance and limited number of effective drugs now available underline how important it is to discover new antimalarial compounds. In the present study, ten plants were extracted with ethyl acetate and methanol and tested for their antimalarial activity against chloroquine (CQ)-sensitive (3D7) and CQ-resistant (Dd2 and INDO) strains of Plasmodium falciparum in culture using the fluorescence-based SYBR Green assay. Plant extracts showed moderate to good antiparasitic effects. Promising antiplasmodial activity was found in the extracts from two plants, Phyllanthus emblica leaf 50% inhibitory concentration (IC₅₀) 3D7: 7.25 μg/mL (ethyl acetate extract), 3.125 μg/mL (methanol extract), and Syzygium aromaticum flower bud, IC₅₀ 3D7:13 μg/mL, (ethyl acetate extract) and 6.25 μg/mL (methanol extract). Moderate activity (30-75 μg/mL) was found in the ethyl acetate and methanol extracts of Abrus precatorius (seed) and Gloriosa superba (leaf); leaf ethyl acetate extracts of Annona squamosa and flower of Musa paradisiaca. The above mentioned plant extracts were also found to be active against CQ-resistant strains (Dd2 and INDO). Cytotoxicity study with P. emblica leaf and S. aromaticum flower bud, extracts showed good therapeutic indices. These results demonstrate that leaf ethyl acetate and methanol extracts of P. emblica and flower bud extract of S. aromaticum may serve as antimalarial agents even in their crude form. The isolation of compounds from P. emblica and S. aromaticum seems to be of special interest for further antimalarial studies.

  6. Antinociceptive action of (+/-)-cis-(6-ethyl-tetrahydropyran-2-yl)-formic acid in mice.

    PubMed

    Marinho, Bruno G; Miranda, Leandro S M; Gomes, Niele M; Matheus, Maria Eline; Leitão, Suzana G; Vasconcellos, Mario Luiz A A; Fernandes, Patrícia D

    2006-11-21

    The objective of this study was to investigate spinal and supraspinal antinociceptive effects of a new synthetic compound, (+/-)-cis-(6-ethyl-tetrahydropyran-2-yl)-formic acid (tetrahydropyran derivative). Its activity was compared with those from morphine. In peripheral models of inflammation and hyperalgesia, tetrahydropyran derivative significantly reduced nociceptive effect induced by acetic acid or formalin in mice. Tetrahydropyran derivative developed antinociceptive effect on the tail-flick and hot-plate tests with a long-acting curve maintaining the effect for 4 h longer than morphine. The opioid receptor antagonist naloxone totally reverted tetrahydropyran derivative effects on both models. Morphine as well as tetrahydropyran derivative induced tolerance and sedation in mice. However, tetrahydropyran derivative-induced tolerance had its onset retarded and the sedative activity was lower when compared to that induced by morphine. These results indicate that this new substance develops an antinociceptive activity and may be used in the future as a substitute for traditional opioids.

  7. Alisol B 23-acetate protects against non-alcoholic steatohepatitis in mice via farnesoid X receptor activation

    PubMed Central

    Meng, Qiang; Duan, Xing-ping; Wang, Chang-yuan; Liu, Zhi-hao; Sun, Peng-yuan; Huo, Xiao-kui; Sun, Hui-jun; Peng, Jin-yong; Liu, Ke-xin

    2017-01-01

    Alisol B 23-acetate (AB23A) is a natural triterpenoid isolated from the traditional Chinese medicine rhizoma alismatis, which exhibits a number of pharmacological activities, including anti-hepatitis virus, anti-cancer and antibacterial effects. In this study we examined whether AB23A protected against non-alcoholic steatohepatitis (NASH) in mice, and the mechanisms underlying the protective effects. NASH was induced in mice fed a methionine and choline-deficient (MCD) diet for 4 weeks. The mice were simultaneously treated with AB23A (15, 30, and 60 mg·kg−1·d−1, ig) for 4 weeks. On the last day, blood samples and livers were collected. Serum liver functional enzymes, inflammatoru markers were assessed. The livers were histologically examined using H&E, Oil Red O, Masson's trichrome and Sirius Red staining. Mouse primary hepatocytes were used for in vitro experiments. The mechanisms underlying AB23A protection were analyzed using siRNA, qRT-PCR, and Western blot assays. AB23A treatment significantly and dose-dependently decreased the elevated levels of serum ALT and AST in MCD diet-fed mice. Furthermore, AB23A treatment significantly reduced hepatic triglyceride accumulation, inflammatory cell infiltration and hepatic fibrosis in the mice. AB23A-induced decreases in serum and hepatic lipids were related to decreased hepatic lipogenesis through decreasing hepatic levels of SREBP-1c, FAS, ACC1 and SCD1 and increased lipid metabolism via inducing PPARα, CPT1α, ACADS and LPL. The reduction in inflammatory cell infiltration corresponded to deceased serum levels of mKC and MCP-1 and decreased hepatic gene expression of MCP-1 and VCAM-1. The reduction in hepatic fibrosis was correlated with decreased hepatic gene expression of fibrosis markers. The protective effects of AB23A were FXR-dependent, because treatment with the FXR agonist CDCA mimicked AB23A-induced hepato-protection in the mice, whereas co-administration of FXR antagonist guggulsterone abrogated AB23A

  8. Apoptotic effect of ethyl-4-isothiocyanatobutanoate is associated with DNA damage, proteasomal activity and induction of p53 and p21cip1/waf1.

    PubMed

    Bodo, Juraj; Jakubikova, Jana; Chalupa, Ivan; Bartosova, Zdena; Horakova, Katarina; Floch, Lubomir; Sedlak, Jan

    2006-08-01

    The effect of synthetic isothiocyanate ethyl-4-isothiocyanatobutanoate (E-4IB) on survival of mismatch repair-proficient TK6 and -deficient MT1 cell lines as well as the influence of proteasomal inhibitor MG132, caspase inhibitor Z-VAD-fmk, and ATM inhibitor caffeine on E-4IB modulation of cell cycle and apoptosis was evaluated. Flow cytometric analyses of DNA double strand breaks (gamma-H2AX), mitotic fraction (phospho-histone H3), cell cycle modulation, apoptosis induction (sub-G(0) fraction and fluorescein diacetate staining), and dissipation of transmembrane mitochondrial potential (JC-1 staining) were performed. Western blotting was used for the evaluation of ERK activation, expression of p53, p21(cip1/waf1) and GADD45alpha proteins, as well as PARP fragmentation. Analysis of mitotic nuclei was performed for chromosomal aberrations assessment. MT1 cells were more resistant to E-4IB treatment then TK6 cells (IC(50) 8 muM vs. 4 muM). In both cell lines E-4IB treatment induced phosphorylation of H2AX, increase of p53 protein level, phospho-histone H3 staining, and G(2)/M arrest. The sub-G(0) fragmentation was accompanied by PARP degradation, decreased mitochondrial transmembrane potential, and diminished p21(cip1/waf1) protein expression in TK6 cells. Caspase inhibitor Z-VAD-fmk decreased E-4IB induced sub-G(0) fragmentation and extent of apoptosis in TK6 cells, while proteasome inhibitor MG132 increased number of apoptotic cells in both cell lines tested. A number of aberrant metaphases and clastogenic effect of high E-4IB concentration was observed. The synthetic isothiocyanate E-4IB induced DNA strand breaks, increased mitotic fraction and apoptosis potentiated by MG132 inhibitor in both mismatch repair-proficient and -deficient cell lines.

  9. Conformational changes associated with the binding of zinc acetate at the putative active site of XcTcmJ, a cupin from Xanthomonas campestris pv. campestris

    PubMed Central

    Axelrod, Herbert L.; Kozbial, Piotr; McMullan, Daniel; Krishna, S. Sri; Miller, Mitchell D.; Abdubek, Polat; Acosta, Claire; Astakhova, Tamara; Carlton, Dennis; Caruthers, Jonathan; Chiu, Hsiu-Ju; Clayton, Thomas; Deller, Marc C.; Duan, Lian; Elias, Ylva; Feuerhelm, Julie; Grzechnik, Slawomir K.; Grant, Joanna C.; Han, Gye Won; Jaroszewski, Lukasz; Jin, Kevin K.; Klock, Heath E.; Knuth, Mark W.; Kumar, Abhinav; Marciano, David; Morse, Andrew T.; Murphy, Kevin D.; Nigoghossian, Edward; Okach, Linda; Oommachen, Silvya; Paulsen, Jessica; Reyes, Ron; Rife, Christopher L.; Tien, Henry J.; Trout, Christina V.; van den Bedem, Henry; Weekes, Dana; White, Aprilfawn; Xu, Qingping; Zubieta, Chloe; Hodgson, Keith O.; Wooley, John; Elsliger, Marc-André; Deacon, Ashley M.; Godzik, Adam; Lesley, Scott A.; Wilson, Ian A.

    2010-01-01

    In the plant pathogen Xanthomonas campestris pv. campestris, the product of the tcmJ gene, XcTcmJ, encodes a protein belonging to the RmlC family of cupins. XcTcmJ was crystallized in a monoclinic space group (C2) in the presence of zinc acetate and the structure was determined to 1.6 Å resolution. Previously, the apo structure has been reported in the absence of any bound metal ion [Chin et al. (2006 ▶), Proteins, 65, 1046–1050]. The most significant difference between the apo structure and the structure of XcTcmJ described here is a reorganization of the binding site for zinc acetate, which was most likely acquired from the crystallization solution. This site is located in the conserved metal ion-binding domain at the putative active site of XcTcmJ. In addition, an acetate was also bound within coordination distance of the zinc. In order to accommodate this binding, rearrangement of a conserved histidine ligand is required as well as several nearby residues within and around the putative active site. These observations indicate that binding of zinc serves a functional role in this cupin protein. PMID:20944231

  10. Conformational changes associated with the binding of zinc acetate at the putative active site of XcTcmJ, a cupin from Xanthomonas campestris pv. campestris.

    PubMed

    Axelrod, Herbert L; Kozbial, Piotr; McMullan, Daniel; Krishna, S Sri; Miller, Mitchell D; Abdubek, Polat; Acosta, Claire; Astakhova, Tamara; Carlton, Dennis; Caruthers, Jonathan; Chiu, Hsiu Ju; Clayton, Thomas; Deller, Marc C; Duan, Lian; Elias, Ylva; Feuerhelm, Julie; Grzechnik, Slawomir K; Grant, Joanna C; Han, Gye Won; Jaroszewski, Lukasz; Jin, Kevin K; Klock, Heath E; Knuth, Mark W; Kumar, Abhinav; Marciano, David; Morse, Andrew T; Murphy, Kevin D; Nigoghossian, Edward; Okach, Linda; Oommachen, Silvya; Paulsen, Jessica; Reyes, Ron; Rife, Christopher L; Tien, Henry J; Trout, Christina V; van den Bedem, Henry; Weekes, Dana; White, Aprilfawn; Xu, Qingping; Zubieta, Chloe; Hodgson, Keith O; Wooley, John; Elsliger, Marc André; Deacon, Ashley M; Godzik, Adam; Lesley, Scott A; Wilson, Ian A

    2010-10-01

    In the plant pathogen Xanthomonas campestris pv. campestris, the product of the tcmJ gene, XcTcmJ, encodes a protein belonging to the RmlC family of cupins. XcTcmJ was crystallized in a monoclinic space group (C2) in the presence of zinc acetate and the structure was determined to 1.6 Å resolution. Previously, the apo structure has been reported in the absence of any bound metal ion [Chin et al. (2006), Proteins, 65, 1046-1050]. The most significant difference between the apo structure and the structure of XcTcmJ described here is a reorganization of the binding site for zinc acetate, which was most likely acquired from the crystallization solution. This site is located in the conserved metal ion-binding domain at the putative active site of XcTcmJ. In addition, an acetate was also bound within coordination distance of the zinc. In order to accommodate this binding, rearrangement of a conserved histidine ligand is required as well as several nearby residues within and around the putative active site. These observations indicate that binding of zinc serves a functional role in this cupin protein.

  11. Synergistic antibacterial activity of Salvia officinalis and Cichorium intybus extracts and antibiotics.

    PubMed

    Stefanović, Olgica D; Stanojević, Dragana D; Comić, Ljiljana R

    2012-01-01

    Synergistic activity of Salvia officinalis and Cichorium intybus extracts and commonly used antibiotics, amoxicillin and chloramphenicol, were evaluated. Interactions between plant extracts and antibiotics were tested by checkerboard method and interpreted as FIC index. Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853 and clinical isolates Staphylococcus aureus, Bacillus subtilis, Enterobacter cloacae, Klebsiella pneumoniae, Escherichia coli and Proteus mirabilis were used. Salvia officinalis showed better synergistic capacity than Cichorium intybus. Synergistic interactions were observed between amoxicillin and acetone or ethyl acetate extract of Salvia officinalis and between chloramphenicol and ethyl acetate extract of Salvia officinalis. In the presence of sub-inhibitory concentration (1/4 MIC to 1/32 MIC) of sage extracts, the MIC values of antibiotics were decreased by 2- to 10-fold. Synergism was observed against all test bacteria, except Escherichia coli. The combinations of acetone and ethyl acetate extract from Cichorium intybus and antibiotics resulted in additive and indifferent effects against tested bacteria.

  12. Effect of increased yeast alcohol acetyltransferase activity on flavor profiles of wine and distillates.

    PubMed

    Lilly, M; Lambrechts, M G; Pretorius, I S

    2000-02-01

    The distinctive flavor of wine, brandy, and other grape-derived alcoholic beverages is affected by many compounds, including esters produced during alcoholic fermentation. The characteristic fruity odors of the fermentation bouquet are primarily due to a mixture of hexyl acetate, ethyl caproate (apple-like aroma), iso-amyl acetate (banana-like aroma), ethyl caprylate (apple-like aroma), and 2-phenylethyl acetate (fruity, flowery flavor with a honey note). The objective of this study was to investigate the feasibility of improving the aroma of wine and distillates by overexpressing one of the endogenous yeast genes that controls acetate ester production during fermentation. The synthesis of acetate esters by the wine yeast Saccharomyces cerevisiae during fermentation is ascribed to at least three acetyltransferase activities, namely, alcohol acetyltransferase (AAT), ethanol acetyltransferase, and iso-amyl AAT. To investigate the effect of increased AAT activity on the sensory quality of Chenin blanc wines and distillates from Colombar base wines, we have overexpressed the alcohol acetyltransferase gene (ATF1) of S. cerevisiae. The ATF1 gene, located on chromosome XV, was cloned from a widely used commercial wine yeast strain of S. cerevisiae, VIN13, and placed under the control of the constitutive yeast phosphoglycerate kinase gene (PGK1) promoter and terminator. Chromoblot analysis confirmed the integration of the modified copy of ATF1 into the genome of three commercial wine yeast strains (VIN7, VIN13, and WE228). Northern blot analysis indicated constitutive expression of ATF1 at high levels in these yeast transformants. The levels of ethyl acetate, iso-amyl acetate, and 2-phenylethyl acetate increased 3- to 10-fold, 3.8- to 12-fold, and 2- to 10-fold, respectively, depending on the fermentation temperature, cultivar, and yeast strain used. The concentrations of ethyl caprate, ethyl caprylate, and hexyl acetate only showed minor changes, whereas the acetic acid

  13. Functional Dissection of the Bipartite Active Site of the Class I Coenzyme A (CoA)-Transferase Succinyl-CoA:Acetate CoA-Transferase

    PubMed Central

    Murphy, Jesse R.; Mullins, Elwood A.; Kappock, T. Joseph

    2016-01-01

    Coenzyme A (CoA)-transferases catalyze the reversible transfer of CoA from acyl-CoA thioesters to free carboxylates. Class I CoA-transferases produce acylglutamyl anhydride intermediates that undergo attack by CoA thiolate on either the internal or external carbonyl carbon atoms, forming distinct tetrahedral intermediates <3 Å apart. In this study, crystal structures of succinyl-CoA:acetate CoA-transferase (AarC) from Acetobacter aceti are used to examine how the Asn347 carboxamide stabilizes the internal oxyanion intermediate. A structure of the active mutant AarC-N347A bound to CoA revealed both solvent replacement of the missing contact and displacement of the adjacent Glu294, indicating that Asn347 both polarizes and orients the essential glutamate. AarC was crystallized with the nonhydrolyzable acetyl-CoA (AcCoA) analog dethiaacetyl-CoA (1a) in an attempt to trap a closed enzyme complex containing a stable analog of the external oxyanion intermediate. One active site contained an acetylglutamyl anhydride adduct and truncated 1a, an unexpected result hinting at an unprecedented cleavage of the ketone moiety in 1a. Solution studies confirmed that 1a decomposition is accompanied by production of near-stoichiometric acetate, in a process that seems to depend on microbial contamination but not AarC. A crystal structure of AarC bound to the postulated 1a truncation product (2a) showed complete closure of one active site per dimer but no acetylglutamyl anhydride, even with acetate added. These findings suggest that an activated acetyl donor forms during 1a decomposition; a working hypothesis involving ketone oxidation is offered. The ability of 2a to induce full active site closure furthermore suggests that it subverts a system used to impede inappropriate active site closure on unacylated CoA. PMID:27242998

  14. Functional dissection of the bipartite active site of the class I coenzyme A (CoA)-transferase succinyl-CoA:acetate CoA-transferase

    NASA Astrophysics Data System (ADS)

    Murphy, Jesse; Mullins, Elwood; Kappock, T.

    2016-05-01

    Coenzyme A (CoA)-transferases catalyze the reversible transfer of CoA from acyl-CoA thioesters to free carboxylates. Class I CoA-transferases produce acylglutamyl anhydride intermediates that undergo attack by CoA thiolate on either the internal or external carbonyl carbon atoms, forming distinct tetrahedral intermediates less than 3 Å apart. In this study, crystal structures of succinyl-CoA:acetate CoA-transferase (AarC) from Acetobacter aceti are used to examine how the Asn347 carboxamide stabilizes the internal oxyanion intermediate. A structure of the active mutant AarC-N347A bound to CoA revealed both solvent replacement of the missing contact and displacement of the adjacent Glu294, indicating that Asn347 both polarizes and orients the essential glutamate. AarC was crystallized with the nonhydrolyzable acetyl-CoA (AcCoA) analogue dethiaacetyl-CoA (1a) in an attempt to trap a closed enzyme complex containing a stable analogue of the external oxyanion intermediate. One active site contained an acetylglutamyl anhydride adduct and truncated 1a, an unexpected result hinting at an unprecedented cleavage of the ketone moiety in 1a. Solution studies confirmed that 1a decomposition is accompanied by production of near-stoichiometric acetate, in a process that seems to depend on microbial contamination but not AarC. A crystal structure of AarC bound to the postulated 1a truncation product (2a) showed complete closure of one active site per dimer but no acetylglutamyl anhydride, even with acetate added. These findings suggest that an activated acetyl donor forms during 1a decomposition; a working hypothesis involving ketone oxidation is offered. The ability of 2a to induce full active site closure furthermore suggests that it subverts a system used to impede inappropriate active site closure on unacylated CoA.

  15. Functional dissection of the bipartite active site of the class I coenzyme A (CoA)-transferase succinyl-CoA:acetate CoA-transferase

    DOE PAGES

    Murphy, Jesse R.; Mullins, Elwood A.; Kappock, T. Joseph

    2016-05-23

    Coenzyme A (CoA)-transferases catalyze the reversible transfer of CoA from acyl-CoA thioesters to free carboxylates. Class I CoA-transferases produce acylglutamyl anhydride intermediates that undergo attack by CoA thiolate on either the internal or external carbonyl carbon atoms, forming distinct tetrahedral intermediates <3 Å apart. Here in this study, crystal structures of succinyl-CoA:acetate CoA-transferase (AarC) from Acetobacter aceti are used to examine how the Asn347 carboxamide stabilizes the internal oxyanion intermediate. A structure of the active mutant AarC-N347A bound to CoA revealed both solvent replacement of the missing contact and displacement of the adjacent Glu294, indicating that Asn347 both polarizes andmore » orients the essential glutamate. AarC was crystallized with the nonhydrolyzable acetyl-CoA (AcCoA) analog dethiaacetyl-CoA (1a) in an attempt to trap a closed enzyme complex containing a stable analog of the external oxyanion intermediate. One active site contained an acetylglutamyl anhydride adduct and truncated 1a, an unexpected result hinting at an unprecedented cleavage of the ketone moiety in 1a. Solution studies confirmed that 1a decomposition is accompanied by production of near-stoichiometric acetate, in a process that seems to depend on microbial contamination but not AarC. A crystal structure of AarC bound to the postulated 1a truncation product (2a) showed complete closure of one active site per dimer but no acetylglutamyl anhydride, even with acetate added. These findings suggest that an activated acetyl donor forms during 1a decomposition; a working hypothesis involving ketone oxidation is offered. Finally, the ability of 2a to induce full active site closure furthermore suggests that it subverts a system used to impede inappropriate active site closure on unacylated CoA.« less

  16. Functional dissection of the bipartite active site of the class I coenzyme A (CoA)-transferase succinyl-CoA:acetate CoA-transferase

    SciTech Connect

    Murphy, Jesse R.; Mullins, Elwood A.; Kappock, T. Joseph

    2016-05-23

    Coenzyme A (CoA)-transferases catalyze the reversible transfer of CoA from acyl-CoA thioesters to free carboxylates. Class I CoA-transferases produce acylglutamyl anhydride intermediates that undergo attack by CoA thiolate on either the internal or external carbonyl carbon atoms, forming distinct tetrahedral intermediates <3 Å apart. Here in this study, crystal structures of succinyl-CoA:acetate CoA-transferase (AarC) from Acetobacter aceti are used to examine how the Asn347 carboxamide stabilizes the internal oxyanion intermediate. A structure of the active mutant AarC-N347A bound to CoA revealed both solvent replacement of the missing contact and displacement of the adjacent Glu294, indicating that Asn347 both polarizes and orients the essential glutamate. AarC was crystallized with the nonhydrolyzable acetyl-CoA (AcCoA) analog dethiaacetyl-CoA (1a) in an attempt to trap a closed enzyme complex containing a stable analog of the external oxyanion intermediate. One active site contained an acetylglutamyl anhydride adduct and truncated 1a, an unexpected result hinting at an unprecedented cleavage of the ketone moiety in 1a. Solution studies confirmed that 1a decomposition is accompanied by production of near-stoichiometric acetate, in a process that seems to depend on microbial contamination but not AarC. A crystal structure of AarC bound to the postulated 1a truncation product (2a) showed complete closure of one active site per dimer but no acetylglutamyl anhydride, even with acetate added. These findings suggest that an activated acetyl donor forms during 1a decomposition; a working hypothesis involving ketone oxidation is offered. Finally, the ability of 2a to induce full active site closure furthermore suggests that it subverts a system used to impede inappropriate active site closure on unacylated CoA.

  17. Organic reactions catalyzed by methylrhenium trioxide: Reactions of ethyl diazoacetate and organic azides

    SciTech Connect

    Zhu, Z.; Espenson, J.H. |

    1996-10-16

    Methylrhenium trioxide (CH{sub 3}ReO{sub 3} or MTO) catalyzes several classes of reactions of ethyl diazoacetate, EDA. It is the first high valent oxo complex for carbene transfer. Under mild conditions and in the absence of other substrates, EDA was converted to a 9:1 mixture of diethyl maleate and diethyl fumarate. In the presence of alcohols, {alpha}-alkoxy ethyl acetates were obtained in good yield. The yields dropped for the larger and more branched alcohols, the balance of material being diethyl maleate and fumarate. An electron-donating group in the para position of phenols favors the formation of {alpha}-phenoxy ethyl acetates. The use of EDA to form {alpha}-thio ethyl acetates and N-substituted glycine ethyl esters, on the other hand, is hardly affected by the size or structure of the parent thiol or amine, with all of these reactions proceeding in high yield. MTO-catalyzed cycloaddition reactions occur between EDA and aromatic imines, olefins, and carbonyl compounds. Three-membered ring products are formed: aziridines, cyclopropanes, and epoxides, respectively. The reactions favor the formation of trans products, and provide a convenient route for the preparation of aziridines. Intermediate carbenoid and nitrenoid species have been proposed. In the presence of an oxygen source such as an epoxide, ethyl diazoacetate and azibenzil are converted to an oxalic acid monoethyl ester and to benzil; at the same time the epoxide was converted to an olefin. 75 refs., 1 fig., 7 tabs.

  18. Larvicidal activity of medicinal plant extracts against Anopheles subpictus & Culex tritaeniorhynchus

    PubMed Central

    Kamaraj, C.; Bagavan, A.; Elango, G.; Zahir, A. Abduz; Rajakumar, G.; Marimuthu, S.; Santhoshkumar, T.; Rahuman, A. Abdul

    2011-01-01

    Background & objectives: Mosquitoes transmit serious human diseases, causing millions of deaths every year and the development of resistance to chemical insecticides resulting in rebounding vectorial capacity. Plants may be alternative sources of mosquito control agents. The present study assessed the role of larvicidal activities of hexane, chloroform, ethyl acetate, acetone, and methanol dried leaf and bark extracts of Annona squamosa L., Chrysanthemum indicum L., and Tridax procumbens L. against the fourth instar larvae of malaria vector, Anopheles subpictus Grassi and Japanese encephalitis vector, Culex tritaeniorhynchus Giles (Diptera: Culicidae). Methods: Larvicidal activities of three medicinal plant extracts were studied in the range of 4.69 to 1000 mg/l in the laboratory bioassays against early 4th instar larvae of An. subpictus and Cx. tritaeniorhynchus. The mortality data were subjected to probit analysis to determine the lethal concentrations (LC50 and LC90) to kill 50 and 90 per cent of the treated larvae of the respective species. Results: All plant extracts showed moderate effects after 24 h of exposure; however, the highest toxic effect of bark methanol extract of A. squamosa, leaf ethyl acetate extract of C. indicum and leaf acetone extract of T. procumbens against the larvae of An. subpictus (LC50 = 93.80, 39.98 and 51.57 mg/l) and bark methanol extract of A. squamosa, leaf methanol extract of C. indicum and leaf ethyl acetate extract of T. procumbens against the larvae of Cx. tritaeniorhynchus (LC50 =104.94, 42.29 and 69.16 mg/l) respectively. Interpretation & Conclusions: Our data suggest that the bark ethyl acetate and methanol extract of A. squamosa, leaf ethyl acetate and methanol extract of C. indicum, acetone and ethyl acetate extract of T. procumbens have the potential to be used as an ecofriendly approach for the control of the An. subpictus, and Cx. tritaeniorhynchus. PMID:21808141

  19. Lipid peroxidation inhibition and antiradical activities of some leaf fractions of Mangifera indica.

    PubMed

    Badmus, Jelili A; Adedosu, Temitope O; Fatoki, John O; Adegbite, Victor A; Adaramoye, Oluwatosin A; Odunola, Oyeronke A

    2011-01-01

    This study was undertaken to assess in vitro lipid peroxidation inhibitions and anti-radical activities of methanolic, chloroform, ethyl acetate and water fractions of Mangifera indica leaf. Inhibition of Fe(2+)-induced lipid peroxidation (LPO) in egg, brain, and liver homogenates, 1,1-diphenyl-2-picrylhydrazyl (DPPH) and hydroxyl (OH-) radical scavenging activities were evaluated. Total phenol was assessed in all fractions, and the reducing power of methanolic fraction was compared to gallic acid and ascorbic acid. The results showed that Fe2+ induced significant lipid peroxidation (LPO) in all the homogenates. Ethyl acetate fraction showed the highest percentage inhibition of LPO in both egg yolk (68.3%) and brain (66.3%), while the aqueous fraction exerted the highest inhibition in liver homogenate (89.1%) at a concentration of 10 microg/mL. These observed inhibitions of LPO by these fractions were higher than that of ascorbic acid used as a standard. The DPPH radical scavenging ability exhibited by ethyl acetate fraction was found to be the highest with IC50 value of 1.5 microg/mL. The ethyl acetate and methanolic fractions had the highest OH- radical scavenging ability with the same IC50 value of 5 microg/mL. The total phenol content of ethyl acetate fraction was the highest with 0.127 microg/mg gallic acid equivalent (GAE). The reductive potential of methanolic fraction showed a concentration-dependent increase. This study showed that inhibition of LPO and the DPPH and OH- radicals scavenging abilities of Mangifera indica leaf could be related to the presence of phenolic compounds. Therefore, the ethyl acetate fraction of the leaf may be a good source of natural antioxidative agent.

  20. Acetaldehyde partial oxidation on the Au(111) model catalyst surface: C-C bond activation and formation of methyl acetate as an oxidative coupling product

    NASA Astrophysics Data System (ADS)

    Karatok, Mustafa; Vovk, Evgeny I.; Shah, Asad A.; Turksoy, Abdurrahman; Ozensoy, Emrah

    2015-11-01

    Partial oxidation of acetaldehyde (CH3CHO) on the oxygen pre-covered Au(111) single crystal model catalyst was investigated via Temperature Programmed Desorption (TPD) and Temperature Programmed Reaction Spectroscopy (TPRS) techniques, where ozone (O3) was utilized as the oxygen delivery agent providing atomic oxygen to the reacting surface. We show that for low exposures of O3 and small surface oxygen coverages, two partial oxidation products namely, methyl acetate (CH3COOCH3) and acetic acid (CH3COOH) can be generated without the formation of significant quantities of carbon dioxide. The formation of methyl acetate as the oxidative coupling reaction product implies that oxygen pre-covered Au(111) single crystal model catalyst surface can activate C-C bonds. In addition to the generation of these products; indications of the polymerization of acetaldehyde on the gold surface were also observed as an additional reaction route competing with the partial and total oxidation pathways. The interplay between the partial oxidation, total oxidation and polymerization pathways reveals the complex catalytic chemistry associated with the interaction between the acetaldehyde and atomic oxygen on catalytic gold surfaces.

  1. In Vitro and In Vivo Drug-Drug Interaction Studies to Assess the Effect of Abiraterone Acetate, Abiraterone, and Metabolites of Abiraterone on CYP2C8 Activity.

    PubMed

    Monbaliu, Johan; Gonzalez, Martha; Bernard, Apexa; Jiao, James; Sensenhauser, Carlo; Snoeys, Jan; Stieltjes, Hans; Wynant, Inneke; Smit, Johan W; Chien, Caly

    2016-10-01

    Abiraterone acetate, the prodrug of the cytochrome P450 C17 inhibitor abiraterone, plus prednisone is approved for treatment of metastatic castration-resistant prostate cancer. We explored whether abiraterone interacts with drugs metabolized by CYP2C8, an enzyme responsible for the metabolism of many drugs. Abiraterone acetate and abiraterone and its major metabolites, abiraterone sulfate and abiraterone sulfate N-oxide, inhibited CYP2C8 in human liver microsomes, with IC50 values near or below the peak total concentrations observed in patients with metastatic castration-resistant prostate cancer (IC50 values: 1.3-3.0 µM, 1.6-2.9 µM, 0.044-0.15 µM, and 5.4-5.9 µM, respectively). CYP2C8 inhibition was reversible and time-independent. To explore the clinical relevance of the in vitro data, an open-label, single-center study was conducted comprising 16 healthy male subjects who received a single 15-mg dose of the CYP2C8 substrate pioglitazone on day 1 and again 1 hour after the administration of abiraterone acetate 1000 mg on day 8. Plasma concentrations of pioglitazone, its active M-III (keto derivative) and M-IV (hydroxyl derivative) metabolites, and abiraterone were determined for up to 72 hours after each dose. Abiraterone acetate increased exposure to pioglitazone; the geometric mean ratio (day 8/day 1) was 125 [90% confidence interval (CI), 99.9-156] for Cmax and 146 (90% CI, 126-171) for AUClast Exposure to M-III and M-IV was reduced by 10% to 13%. Plasma abiraterone concentrations were consistent with previous studies. These results show that abiraterone only weakly inhibits CYP2C8 in vivo.

  2. Crataegus azarolus Leaves Induce Antiproliferative Activity, Cell Cycle Arrest, and Apoptosis in Human HT-29 and HCT-116 Colorectal Cancer Cells.

    PubMed

    Mustapha, Nadia; Pinon, Aline; Limami, Youness; Simon, Alain; Ghedira, Kamel; Hennebelle, Thierry; Chekir-Ghedira, Leila

    2016-05-01

    Limited success has been achieved in extending the survival of patients with metastatic colorectal cancer (CRC). There is a strong need for novel agents in the treatment and prevention of CRC. Therefore, in the present study we evaluated the antiproliferative and pro-apoptotic potential of Crataegus azarolus ethyl acetate extract in HCT-116 and HT-29 human colorectal cancer cell lines. Moreover, we attempted to investigate the signaling pathways that should be involved in its cytotoxic effect. The Crataegus azarolus ethyl acetate extract-induced growth inhibitory effect was associated with DNA fragmentation, sub-G1 peak, loss of mitochondrial potential, and poly (ADP-ribose) polymerase (PARP) cleavage. In addition, ethyl acetate extract of Crataegus azarolus induced the cleavage of caspase-8. It has no effect on steady-state levels of total Bcl-2 protein. Whereas Bax levels decreased significantly in a dose-dependent manner in both tested cell lines. Taken together, these findings confirm the involvement of the extrinsic pathway of apoptosis. The apoptotic cell death induced by ethyl acetate extract of Crataegus azarolus was accompanied by an enhancement of the p21 expression but not through p53 activation in human colorectal cancer cells. The above-mentioned data provide insight into the molecular mechanisms of Crataegus azarolus ethyl acetate extract-induced apoptosis in CRC. Therefore, this compound should be a potential anticancer agent for the treatment of CRC.

  3. Antinociceptive Effect of Tephrosia sinapou Extract in the Acetic Acid, Phenyl-p-benzoquinone, Formalin, and Complete Freund's Adjuvant Models of Overt Pain-Like Behavior in Mice.

    PubMed

    Martinez, Renata M; Zarpelon, Ana C; Domiciano, Talita P; Georgetti, Sandra R; Baracat, Marcela M; Moreira, Isabel C; Andrei, Cesar C; Verri, Waldiceu A; Casagrande, Rubia

    2016-01-01

    Tephrosia toxicaria, which is currently known as Tephrosia sinapou (Buc'hoz) A. Chev. (Fabaceae), is a source of compounds such as flavonoids. T. sinapou has been used in Amazonian countries traditional medicine to alleviate pain and inflammation. The purpose of this study was to evaluate the analgesic effects of T. sinapou ethyl acetate extract in overt pain-like behavior models in mice by using writhing response and flinching/licking tests. We demonstrated in this study that T. sinapou extract inhibited, in a dose (1-100 mg/kg) dependent manner, acetic acid- and phenyl-p-benzoquinone- (PBQ-) induced writhing response. Furthermore, it was active via intraperitoneal, subcutaneous, and peroral routes of administration. T. sinapou extract also inhibited formalin- and complete Freund's adjuvant- (CFA-) induced flinching/licking at 100 mg/kg dose. In conclusion, these findings demonstrate that T. sinapou ethyl acetate extract reduces inflammatory pain in the acetic acid, PBQ, formalin, and CFA models of overt pain-like behavior. Therefore, the potential of analgesic activity of T. sinapou indicates that it deserves further investigation.

  4. Antinociceptive Effect of Tephrosia sinapou Extract in the Acetic Acid, Phenyl-p-benzoquinone, Formalin, and Complete Freund's Adjuvant Models of Overt Pain-Like Behavior in Mice

    PubMed Central

    Martinez, Renata M.; Zarpelon, Ana C.; Domiciano, Talita P.; Georgetti, Sandra R.; Baracat, Marcela M.; Moreira, Isabel C.; Andrei, Cesar C.; Verri, Waldiceu A.; Casagrande, Rubia

    2016-01-01

    Tephrosia toxicaria, which is currently known as Tephrosia sinapou (Buc'hoz) A. Chev. (Fabaceae), is a source of compounds such as flavonoids. T. sinapou has been used in Amazonian countries traditional medicine to alleviate pain and inflammation. The purpose of this study was to evaluate the analgesic effects of T. sinapou ethyl acetate extract in overt pain-like behavior models in mice by using writhing response and flinching/licking tests. We demonstrated in this study that T. sinapou extract inhibited, in a dose (1–100 mg/kg) dependent manner, acetic acid- and phenyl-p-benzoquinone- (PBQ-) induced writhing response. Furthermore, it was active via intraperitoneal, subcutaneous, and peroral routes of administration. T. sinapou extract also inhibited formalin- and complete Freund's adjuvant- (CFA-) induced flinching/licking at 100 mg/kg dose. In conclusion, these findings demonstrate that T. sinapou ethyl acetate extract reduces inflammatory pain in the acetic acid, PBQ, formalin, and CFA models of overt pain-like behavior. Therefore, the potential of analgesic activity of T. sinapou indicates that it deserves further investigation. PMID:27293981

  5. Correlation between chemical structure, receptor binding, and biological activity of some novel, highly active, 16 alpha, 17 alpha-acetal-substituted glucocorticoids.

    PubMed

    Dahlberg, E; Thalén, A; Brattsand, R; Gustafsson, J A; Johansson, U; Roempke, K; Saartok, T

    1984-01-01

    The affinity for the glucocorticoid receptor in rat skeletal muscle of some glucocorticoids with a new type of 16 alpha, 17 alpha-acetal substituent has been estimated and correlated to the glucocorticoid activities in three in vivo systems in rats. Budesonide (an approximately 1:1 mixture of the C(22) epimers of 11 beta, 21-dihydroxy-16 alpha, 17 alpha-[(22R,S)-propylmethylenedioxy]-pregna-1,4-diene-3,20-dione) and the isolated (22R)- and (22S)-epimers bound to the same binding site as the potent glucocorticoids dexamethasone (DEX) or triamcinolone 16 alpha, 17 alpha-acetonide (TA), but with even higher affinity than DEX or TA, despite the lack of a 9 alpha-fluoro atom in budesonide and its epimers. The (22R)-epimer was twice as active as the (22S)-epimer, 4 times more active than TA, and 14 times more active than DEX. The introduction of a 9 alpha-fluoro atom slightly decreased the binding affinity of the (22R)-epimer of budesonide, in contrast to the positive effect of 9 alpha-fluorination of, e.g., 16 alpha, 17 alpha-acetonides. The negative influence of 9 alpha-fluorination of the (22R)-epimer was partially reversed in the 6 alpha, 9 alpha-difluorinated (22R)-epimer. Nevertheless, the fluorinated compounds were more active than DEX and TA (8 and 11 times more active than DEX, and 2 and 3 times more active than TA, in case of the 9 alpha-fluoro- and 6 alpha, 9 alpha-difluoro-derivatives of the (22R)-epimer, respectively). Budesonide is metabolized mainly to 16 alpha-hydroxyprednisolone (11 beta, 16 alpha, 17 alpha, 21-tetrahydroxy-pregna-1,4-diene-3,20-dione) and 6 beta-hydroxy-budesonide. Both metabolites were very weak competitors for the ligand-binding sites on the receptor (3% and 6% of the affinity of DEX, respectively). The affinity for the receptor in vitro was closely correlated to the topical glucocorticoid activity in vivo for the 12 steroids compared (r = 0.98; R = 0.98), which supports the contention that in vitro tests for receptor affinity are

  6. Antimicrobial Activity and Phylogenetic Analysis of Streptomyces Parvulus Dosmb-D105 Isolated from the Mangrove Sediments of Andaman Islands.

    PubMed

    Baskaran, R; Mohan, P M; Sivakumar, K; Kumar, Ashok

    2016-03-01

    Actinomycetes, especially species of Streptomyces are prolific producers of pharmacologically significant compounds accounting for about 70% of the naturally derived antibiotics that are presently in clinical use. In this study, we used five solvents to extract the secondary metabolites from marine Streptomyces parvulus DOSMB-D105, which was isolated from the mangrove sediments of the South Andaman Islands. Among them, ethyl acetate crude extract showed maximum activity against 11 pathogenic bacteria and six fungi. Presence of bioactive compounds in the ethyl acetate extract was determined using GC-MS and the compounds detected in the ethyl acetate extract were matched with the National Institute of Standards and Technology (NIST) library. Totally eight compounds were identified and the prevalent compounds were 2 steroids, 2 alkaloids, 2 plasticizers, 1 phenolic and 1 alkane. Present study revealed that S. parvulus DOSMB-D105 is a promising species for the isolation of valuable bioactive compounds to combat pathogenic microbes.

  7. MOLLUSCICIDAL AND LARVICIDAL ACTIVITIES OF Atriplex inflata AERIAL PARTS AGAINST THE MOLLUSK Galba truncatula, INTERMEDIATE HOST OF Fasciola hepatica.

    PubMed

    Hamed, Néjia; Njeh, Fatma; Damak, Mohamed; Ayadi, Ali; Mezghani-Jarraya, Raoudha; Hammami, Hayet

    2015-12-01

    Fasciolosis is a widespread parasitosis of farm live-stock in many developing countries. For this reason, it is necessary to search for new substances against parasitic diseases caused by flukes. Indeed, a wide variety of terrestrial plants have been subjected to chemical and pharmacological screening in order to discover their potential for human medicinal use. The molluscicidal and larvicidal activities of Atriplex inflata were tested on Galba truncatula and Fasciola hepatica larval stages infecting this snail in Tunisia. Phytochemical tests were conducted on extracts in order to establish a meaningful relationship with molluscicidal and larvicidal activities. The molluscicidal activity was evaluated by subjecting snails to sample aqueous solutions. Accordingly, hexane, ethyl acetate, methanol and methanol-water (8:2, v-v) were used as extraction solvents. As a result, hexane and ethyl acetate extracts showed potent activity, according to the World Health Organization, giving LC50 = 7.59 mg/L and 6.69 mg/L for hexane extracts of leaves and fruits, respectively. Ethyl acetate extracts gave LC50 = 5.90 mg/L and 7.32 mg/L for leaves and fruits, successively. Molluscicidal activities of powders were less potent on snails, but active according to the World Health Organization. Hexane and ethyl acetate extracts from leaves and fruits gave potent larvicidal activities with a delay rate exceeding 45.50% (45.50- 98.92%). Phytochemical tests showed that these activities may be attributed to the presence of triterpenoids and/or sterols.

  8. Quantification of aroma compounds in Parmigiano Reggiano cheese by a dynamic headspace gas chromatography-mass spectrometry technique and calculation of odor activity value.

    PubMed

    Qian, Michael; Reineccius, G A

    2003-03-01

    Potentially important aroma compounds in Parmigiano Reggiano cheese were quantified. Free fatty acids were isolated with ion-exchange chromatography and quantified by gas chromatography. Neutral aroma compounds were quantified with a purge-trap/gas chromatography-mass spectrometry with selective mass ion technique. Odor activity values were calculated based on sensory thresholds reported in literature. The calculated odor activity values suggest that 3-methylbutanal, 2-methylpropanal, 2-methylbutanal, dimethyl trisulfide, diacetyl, methional, phenylacetaldehyde, ethyl butanoate, ethyl hexanoate, ethyl octanoate, acetic, butanoic, hexanoic, and octanoic acids are the most important aroma contributors to Parmigiano Reggiano cheese.

  9. Antioxidant Activity and Gas Chromatographic-Mass Spectrometric Analysis of Extracts of the Marine Algae, Caulerpa peltata and Padina Gymnospora

    PubMed Central

    Murugan, Kavitha; Iyer, Vidhya V.

    2014-01-01

    The results of our previous investigations on extracts of selected marine algae showed that Caulerpa peltata and Padina gymnospora had more promising antiproliferative and antioxidant activities than Gelidiella acerosa and Sargassum wightii. Based on these results, the more active chloroform extract of C. peltata and ethyl acetate extract of P. gymnospora were further analyzed for their constituents by using gas chromatography in tandem with mass spectrometry. The GC-MS analysis (GC % peak area given in parentheses) showed that fucosterol (12.45%) and L-(+)-ascorbic acid 2, 6-dihexadecanoate (8.13%) were the major compounds present in P. gymnospora ethyl acetate extract. On the other hand, C. peltata chloroform extract had 1-heptacosanol (10.52%), hexacosanol acetate (9.28%), tetradecyl ester of chloroacetic acid (7.22%), Z,Z-6, 28-heptatriactontadien-2-one (6.77%) and 10, 13-dimethyl-methyl ester of tetradecanoic acid (5.34%) as major compounds. Also described in the report are the beta-carotene bleaching inhibitory and total reducing activities of the chloroform and ethyl acetate extracts of C. peltata and P. gymnospora, respectively, relative to the other three extracts (aqueous, methanol, chloroform or ethyl acetate) of the two algae. PMID:25593390

  10. The transcription factors ADR1 or CAT8 are required for RTG pathway activation and evasion from yeast acetic acid-induced programmed cell death in raffinose

    PubMed Central

    Laera, Luna; Guaragnella, Nicoletta; Ždralević, Maša; Marzulli, Domenico; Liu, Zhengchang; Giannattasio, Sergio

    2016-01-01

    Yeast Saccharomyces cerevisiae grown on glucose undergoes programmed cell death (PCD) induced by acetic acid (AA-PCD), but evades PCD when grown in raffinose. This is due to concomitant relief of carbon catabolite repression (CCR) and activation of mitochondrial retrograde signaling, a mitochondria-to-nucleus communication pathway causing up-regulation of various nuclear target genes, such as CIT2, encoding peroxisomal citrate synthase, dependent on the positive regulator RTG2 in response to mitochondrial dysfunction. CCR down-regulates genes mainly involved in mitochondrial respiratory metabolism. In this work, we investigated the relationships between the RTG and CCR pathways in the modulation of AA-PCD sensitivity under glucose repression or de-repression conditions. Yeast single and double mutants lacking RTG2 and/or certain factors regulating carbon source utilization, including MIG1, HXK2, ADR1, CAT8, and HAP4, have been analyzed for their survival and CIT2 expression after acetic acid treatment. ADR1 and CAT8 were identified as positive regulators of RTG-dependent gene transcription. ADR1 and CAT8 interact with RTG2 and with each other in inducing cell resistance to AA-PCD in raffinose and controlling the nature of cell death. In the absence of ADR1 and CAT8, AA-PCD evasion is acquired through activation of an alternative factor/pathway repressed by RTG2, suggesting that RTG2 may play a function in promoting necrotic cell death in repressing conditions when RTG pathway is inactive. Moreover, our data show that simultaneous mitochondrial retrograde pathway activation and SNF1-dependent relief of CCR have a key role in central carbon metabolism reprogramming which modulates the yeast acetic acid-stress response. PMID:28357334

  11. In Vitro Toxicity and Activity of Dakin’s Solution, Mafenide Acetate, and Amphotericin B on Filamentous Fungi and Human Cells

    DTIC Science & Technology

    2013-08-01

    clinical or in vitro studies did not include molds, but Dakin’s solution has shown activity against Aspergillus flavus and Aspergillus niger but less...clear bottoms (Fisher, Pittsburgh, PA) were exposed to mafenide acetate, amphotericin B, SMAT, and Dakin’s solutions diluted in saline (0.9% NaCl, pH 7.4...in 1· phosphate-buffered saline , pH 7.4 (Sigma). Toxicity of topical solutions was measured using the CellTiter Flour assay (Promega, Madison, WI) as

  12. Acetic acid treatment in S. cerevisiae creates significant energy deficiency and nutrient starvation that is dependent on the activity of the mitochondrial transcriptional complex Hap2-3-4-5

    PubMed Central

    Kitanovic, Ana; Bonowski, Felix; Heigwer, Florian; Ruoff, Peter; Kitanovic, Igor; Ungewiss, Christin; Wölfl, Stefan

    2012-01-01

    Metabolic pathways play an indispensable role in supplying cellular systems with energy and molecular building blocks for growth, maintenance and repair and are tightly linked with lifespan and systems stability of cells. For optimal growth and survival cells rapidly adopt to environmental changes. Accumulation of acetic acid in stationary phase budding yeast cultures is considered to be a primary mechanism of chronological aging and induction of apoptosis in yeast, which has prompted us to investigate the dependence of acetic acid toxicity on extracellular conditions in a systematic manner. Using an automated computer controlled assay system, we investigated and model the dynamic interconnection of biomass yield- and growth rate-dependence on extracellular glucose concentration, pH conditions and acetic acid concentration. Our results show that toxic concentrations of acetic acid inhibit glucose consumption and reduce ethanol production. In absence of carbohydrates uptake, cells initiate synthesis of storage carbohydrates, trehalose and glycogen, and upregulate gluconeogenesis. Accumulation of trehalose and glycogen, and induction of gluconeogenesis depends on mitochondrial activity, investigated by depletion of the Hap2-3-4-5 complex. Analyzing the activity of glycolytic enzymes, glyceraldehyde-3-phosphate dehydrogenase (GAPDH), pyruvate kinase (PYK), and glucose-6-phosphate dehydrogenase (G6PDH) we found that while high acetic acid concentration increased their activity, lower acetic acids concentrations significantly inhibited these enzymes. With this study we determined growth and functional adjustment of metabolism to acetic acid accumulation in a complex range of extracellular conditions. Our results show that substantial acidification of the intracellular environment, resulting from accumulation of dissociated acetic acid in the cytosol, is required for acetic acid toxicity, which creates a state of energy deficiency and nutrient starvation. PMID:23050242

  13. Acetic acid treatment in S. cerevisiae creates significant energy deficiency and nutrient starvation that is dependent on the activity of the mitochondrial transcriptional complex Hap2-3-4-5.

    PubMed

    Kitanovic, Ana; Bonowski, Felix; Heigwer, Florian; Ruoff, Peter; Kitanovic, Igor; Ungewiss, Christin; Wölfl, Stefan

    2012-01-01

    Metabolic pathways play an indispensable role in supplying cellular systems with energy and molecular building blocks for growth, maintenance and repair and are tightly linked with lifespan and systems stability of cells. For optimal growth and survival cells rapidly adopt to environmental changes. Accumulation of acetic acid in stationary phase budding yeast cultures is considered to be a primary mechanism of chronological aging and induction of apoptosis in yeast, which has prompted us to investigate the dependence of acetic acid toxicity on extracellular conditions in a systematic manner. Using an automated computer controlled assay system, we investigated and model the dynamic interconnection of biomass yield- and growth rate-dependence on extracellular glucose concentration, pH conditions and acetic acid concentration. Our results show that toxic concentrations of acetic acid inhibit glucose consumption and reduce ethanol production. In absence of carbohydrates uptake, cells initiate synthesis of storage carbohydrates, trehalose and glycogen, and upregulate gluconeogenesis. Accumulation of trehalose and glycogen, and induction of gluconeogenesis depends on mitochondrial activity, investigated by depletion of the Hap2-3-4-5 complex. Analyzing the activity of glycolytic enzymes, glyceraldehyde-3-phosphate dehydrogenase (GAPDH), pyruvate kinase (PYK), and glucose-6-phosphate dehydrogenase (G6PDH) we found that while high acetic acid concentration increased their activity, lower acetic acids concentrations significantly inhibited these enzymes. With this study we determined growth and functional adjustment of metabolism to acetic acid accumulation in a complex range of extracellular conditions. Our results show that substantial acidification of the intracellular environment, resulting from accumulation of dissociated acetic acid in the cytosol, is required for acetic acid toxicity, which creates a state of energy deficiency and nutrient starvation.

  14. Chemical constituents and biological activities of Senecio aegyptius var. discoideus Boiss.

    PubMed

    Hassan, Wafaa; Al-Gendy, Amal; Al-Youssef, Hanan; El-Shazely, Assem

    2012-01-01

    A new eremophilane sesquiterpene, 1-beta-hydroxy-8-oxoeremophila-7,9-dien-12-oic acid (1), in addition to two known flavonol glycosides, rutin (2) and quercetin-3-O-glucoside-7-O-rutinoside (3), was isolated from the ethyl acetate fraction obtained from the aqueous alcoholic extract of the aerial parts of Senecio aegyptius var. discoideus Boiss. (family Asteraceae). The chemical structures of the isolated compounds were established by 1D and 2D NMR analysis (1H, 13C, COSY, HMQC, HMBC), MS and UV data, and through comparison with the literature. The ethyl acetate fraction and the isolated rutin showed significant cytotoxic activity against colorectal carcinoma (HCT 116) and to less extent against brain (U 251) and breast carcinoma (MCF 7). The ethyl acetate fraction showed a significant level of activity against Klebsiella pneumoniae, while the total extract showed the best antifungal activity against Candida albicans and Saccharomyces cerevisiae. DPPH radical scavenging activity of the ethyl acetate fraction was significant (96.7%) when compared to ascorbic acid. It also showed anti-inflammatory activity but no diuretic effect.

  15. Citrate and the conversion of carbohydrate in fat. The activities of citrate-cleavage enzyme and acetate thiokinase in livers of starved and re-fed rats

    PubMed Central

    Kornacker, Melodee S.; Lowenstein, J. M.

    1965-01-01

    1. The activity of citrate-cleavage enzyme varies in accordance with the nutritional state of the animal. It is suppressed on starvation and restored on re-feeding after starvation. 2. The increase in enzyme activity that occurs on re-feeding starved animals depends on the diet. It is largest on diets high in carbohydrate and low in fat, and smallest on diets high in fat. Intermediate increases are obtained with balanced diets. 3. The ratio of activities of citrate-cleavage enzyme to acetate thiokinase varies from 2·5 for animals maintained on a balanced diet to 20 for animals re-fed with a diet high in carbohydrate. 4. The changes in activity of citrate-cleavage enzyme correlate with changes in the rate of fatty acid synthesis and provide evidence for the involvement of the citrate-cleavage reaction in fatty acid synthesis. PMID:14342232

  16. In vitro antimicrobial activity of four Ficus carica latex fractions against resistant human pathogens (antimicrobial activity of Ficus carica latex).

    PubMed

    Aref, Houda Lazreg; Salah, Karima Bel Hadj; Chaumont, Jean Pierre; Fekih, Abdelwaheb; Aouni, Mahjoub; Said, Khaled

    2010-01-01

    Methanolic, hexanoïc, chloroformic and ethyl acetate extracts of Ficus carica latex were investigated for their in vitro antimicrobial proprieties against five bacteria species and seven strains of fungi. The green fruit latex was collected from Chott Mariam Souse, Middle East coast of Tunisia. The antimicrobial activity of the extracts was evaluated and based respectively on the inhibition zone using the disc-diffusion assay, minimal inhibition concentration (MIC) for bacterial testing and the method by calculating inhibition percentage (I%) for fungi-inhibiting activities. The methanolic extract had no effect against bacteria except for Proteus mirabilis while the ethyl acetate extract had inhibition effect on the multiplication of five bacteria species (Enterococcus fecalis, Citobacter freundei, Pseudomonas aeruginosa, Echerchia coli and Proteus mirabilis). For the opportunist pathogenic yeasts, ethyl acetate and chlorophormic fractions showed a very strong inhibition (100%); methanolic fraction had a total inhibition against Candida albicans (100%) at a concentration of 500 microg/ml and a negative effect against Cryptococcus neoformans. Microsporum canis was strongly inhibited with methanolic extract (75%) and totally with ethyl acetate extract at a concentration of 750 microg/ml. Hexanoïc extract showed medium results.

  17. CO2 capture in ionic liquid 1-alkyl-3-methylimidazolium acetate: a concerted mechanism without carbene.

    PubMed

    Yan, Fangyong; Dhumal, Nilesh R; Kim, Hyung J

    2017-01-04

    Ionic liquids (ILs) provide a promising medium for CO2 capture. Recently, the family of ILs comprising imidazolium-based cations and acetate anions, such as 1-ethyl-3-methylimidazolium acetate (EMI(+)OAc(-)), has been found to react with CO2 and form carboxylate compounds. N-Heterocyclic carbene (NHC) is widely assumed to be responsible by directly reacting with CO2 though NHC has not been detected in these ILs. Herein, a computational analysis of CO2 capture in EMI(+)OAc(-) is presented. Quantum chemistry calculations predict that NHC is unstable in a polar environment, suggesting that NHC is not formed in EMI(+)OAc(-). Ab initio molecular dynamics simulations indicate that an EMI(+) ion "activated" by the approach of a CO2 molecule can donate its acidic proton to a neighboring OAc(-) anion and form a carboxylate compound with the CO2 molecule. Analysis of this termolecular process indicates that the EMI(+)-to-OAc(-) proton transfer and the formation of 1-ethyl-3-methylimidazolium-2-carboxylate occur essentially concurrently. Based on these findings, a novel concerted mechanism that does not involve NHC is proposed for CO2 capture.

  18. Synthesis and activity of novel 16-dehydropregnenolone acetate derivatives as inhibitors of type 1 5α-reductase and on cancer cell line SK-LU-1.

    PubMed

    Silva-Ortiz, Aylin Viviana; Bratoeff, Eugene; Ramírez-Apan, Teresa; Heuze, Yvonne; Sánchez, Araceli; Soriano, Juan; Cabeza, Marisa

    2015-12-15

    Testosterone (T) plays a crucial role in prostate growth. In androgen-dependent tissues T is reduced to dihydrotestosterone (DHT) because of the presence of the 5α-reductase enzyme. This androgen is more active than T, since it has a higher affinity for the androgen receptor (AR). When this mechanism is altered, androgen-dependent diseases, including prostate cancer, could result. The aim of this study was to synthesize several 16-dehydropregnenolone acetate derivatives containing a triazole ring at C-21 and a linear or alicyclic ester moiety at C-3 of the steroidal skeleton. These steroids were designed as potential inhibitors of the activity of both types (1 and 2) of 5α-reductase. The cytotoxic activity of these compounds was also evaluated on a panel of PC-3, MCF7, and SK-LU-1 human cancer cell lines. The results from this study showed that with the exception of steroids 20-oxo-21-(1H-1,2,4-triazole-1-yl)pregna-5,16-dien-3β-yl-propionate and 20-oxo-21-(1H-1,2,4-triazole-1-yl)pregna-5,16-dien-3β-yl-pentanoate, the compounds exhibit a lower inhibitory activity for both isoenzymes of 5α-reductase than finasteride. Furthermore the 3β-hydroxy-21-(1H-1,2,4-triazole-1-yl)pregna-5,16-dien-20-one and 20-oxo-21-(1H-1,2,4-triazole-1-yl)pregna-5,16-dien-3β-yl-acetate derivatives display 80% cytotoxic activity on the SK-LU-1 cell line. These results also indicated that the triazole derivatives, which have a hydroxyl or acetoxy group at C-3, could have an anticancer effect, whereas the derivatives with a alicyclic ester group at C-3 do not show biological activity.

  19. Effect of bovine serum albumin on the synthesis of prostaglandin and incorporation of (/sup 3/H)acetate into platelet-activating factor

    SciTech Connect

    Heinsohn, C.; Polgar, P.; Fishman, J.; Taylor, L.

    1987-09-01

    The binding of fatty acids by bovine serum albumin (BSA) is well documented. However, the interaction between the synthesis of prostaglandins (PGs) and the trapping of arachidonate released from cellular lipid stores is not as well understood. In this communication, we relate the trapping of fatty acids to the synthesis of PGs and the incorporation of (/sup 3/H)acetate into platelet-activating factor (PAF). Our results show that, as determined by radioimmunoassay, BSA inhibits bradykinin (BK) (5 ng/ml) and ionophore A23187 (10 microM)-stimulated synthesis of PGs in human embryo lung fibroblasts (IMR-90) in a concentration-dependent manner. Experiments using prelabel with (/sup 3/H)arachidonate followed by extraction and thin-layer chromatography show that, in the presence of 2 mg/ml BSA, IMR-90 release essentially only fatty acid following stimulation with bradykinin. Little if any prostaglandin and no endoperoxide are detected. In the same experiment, in absence of BSA, about 70% of the released label is detected as prostaglandin. alpha-Cyclodextrin, another trapper of fatty acid, inhibits PG synthesis in much the same way. BSA and alpha-cyclodextrin also inhibit prostacyclin synthesis in endothelial cells derived from the calf pulmonary artery. However, the inhibition of PG synthesis in these cells is not as complete as that in the IMR-90. In contrast to the effect of the trappers on PG synthesis, BSA and alpha-cyclodextrin are observed to potentiate BK- and ionophore-stimulated incorporation of (3H)acetate into PAF in the endothelial cells. The labeled PAF is not released from the cells in either the presence or absence of the trappers, leading us to conclude that BSA causes an increase in acetate-labeled cellular PAF by trapping released fatty acid.

  20. Molluscicidal activity against Oncomelania hupensis of Ginkgo biloba.

    PubMed

    Yang, Xiao-Ming; Chen, Sheng-Xia; Xia, Lei; Chen, Jun

    2008-06-01

    In search for molluscicidal active components, petroleum ether, ethyl acetate, ethanol, and water extracts from Ginkgo sarcotesta were evaluated against the snail Oncomelania hupensis. The bioassay-oriented showed that the activity concentrates in the petroleum ether extract (LD(50) 7.81 ppm). Ginkgolic acids, isolated from the petroleum ether extract, exhibited strong molluscicidal activity (LD(50) 1.49 ppm), gingkgolic acid C15:1 having the strongest molluscicidal activity.

  1. Towards further understanding on the antioxidative activities of Prunus persica fruit: a comparative study with four different fractions.

    PubMed

    Dhingra, Naveen; Sharma, Rajesh; Kar, Anand

    2014-11-11

    In the present study we have evaluated the antioxidant activities of different fractions (hexane, ethyl acetate, n-butanol and aqueous fractions) of Prunus persica fruit. For extraction simple warring blender method was employed and total phenolic and flavonoid contents were correlated with different antioxidant activities (total antioxidant, 2,2-diphenyl-1-picrylhydrazyl (DPPH), H2O2 scavenging, superoxide radical scavenging, iron chelating and their reducing power properties). Different in vitro antioxidant studies showed that ethyl acetate and n-butanol fractions had the maximum activities that were well correlated with total phenolic and flavonoid contents. Maximum yield (25.14±2.2%) was obtained in its aqueous fraction. Both ethyl acetate and n-butanol fractions showed significant inhibitory effects on different antioxidant activities. A significantly high correlation coefficient existed between total antioxidant activities and with total phenolic as well as total flavonoid contents. It appears that ethyl acetate and n-butanol fractions of P. persica may serve as new potential sources of natural antioxidants and could be of therapeutic use in treating several diseases.

  2. Towards further understanding on the antioxidative activities of Prunus persica fruit: A comparative study with four different fractions

    NASA Astrophysics Data System (ADS)

    Dhingra, Naveen; Sharma, Rajesh; Kar, Anand

    2014-11-01

    In the present study we have evaluated the antioxidant activities of different fractions (hexane, ethyl acetate, n-butanol and aqueous fractions) of Prunus persica fruit. For extraction simple warring blender method was employed and total phenolic and flavonoid contents were correlated with different antioxidant activities (total antioxidant, 2,2-diphenyl-1-picrylhydrazyl (DPPH), H2O2 scavenging, superoxide radical scavenging, iron chelating and their reducing power properties). Different in vitro antioxidant studies showed that ethyl acetate and n-butanol fractions had the maximum activities that were well correlated with total phenolic and flavonoid contents. Maximum yield (25.14 ± 2.2%) was obtained in its aqueous fraction. Both ethyl acetate and n-butanol fractions showed significant inhibitory effects on different antioxidant activities. A significantly high correlation coefficient existed between total antioxidant activities and with total phenolic as well as total flavonoid contents. It appears that ethyl acetate and n-butanol fractions of P. persica may serve as new potential sources of natural antioxidants and could be of therapeutic use in treating several diseases.

  3. 40 CFR 180.585 - Pyraflufen-ethyl; tolerances for residues.

    Code of Federal Regulations, 2014 CFR

    2014-07-01

    ... residues of the herbicide, pyraflufen-ethyl, including its metabolites and degradates, in the commodities...] acetate, and its acid metabolite, E-1, 2-chloro-5-(4-chloro-5-difluoromethoxy-1-methyl-1H-pyrazol-3-yl)-4... metabolites: E-1, 2-chloro-5-(4-chloro-5-difluoromethoxy-1-methyl-1H-pyrazol-3-yl)-4-fluorophenoxyacetic...

  4. 40 CFR 180.585 - Pyraflufen-ethyl; tolerances for residues.

    Code of Federal Regulations, 2013 CFR

    2013-07-01

    ... residues of the herbicide, pyraflufen-ethyl, including its metabolites and degradates, in the commodities...] acetate, and its acid metabolite, E-1, 2-chloro-5-(4-chloro-5-difluoromethoxy-1-methyl-1H-pyrazol-3-yl)-4... metabolites: E-1, 2-chloro-5-(4-chloro-5-difluoromethoxy-1-methyl-1H-pyrazol-3-yl)-4-fluorophenoxyacetic...

  5. Antifungal activity of different neem leaf extracts and the nimonol against some important human pathogens

    PubMed Central

    Mahmoud, D.A.; Hassanein, N.M.; Youssef, K.A.; Abou Zeid, M.A.

    2011-01-01

    This study was conducted to evaluate the effect of aqueous, ethanolic and ethyl acetate extracts from neem leaves on growth of some human pathogens (Aspergillus flavus, Aspergillus fumigatus, Aspergillus niger, Aspergillus terreus, Candida albicans and Microsporum gypseum) in vitro. Different concentrations (5, 10, 15 and 20%) prepared from these extracts inhibited the growth of the test pathogens and the effect gradually increased with concentration. The 20% ethyl acetate extract gave the strongest inhibition compared with the activity obtained by the same concentration of the other extracts. High Performance Liquid Chromatography (HPLC) analysis of ethyl acetate extract showed the presence of a main component (nimonol) which was purified and chemically confirmed by Nuclear Magnetic Resonance (NMR) spectroscopic analysis. The 20% ethyl acetate extract lost a part of its antifungal effect after pooling out the nimonol and this loss in activity was variable on test pathogens. The purified nimonol as a separate compound did not show any antifungal activity when assayed against all the six fungal pathogens. PMID:24031718

  6. Enhancing visible light photocatalytic activity of nitrogen-deficient g-C3N4 via thermal polymerization of acetic acid-treated melamine.

    PubMed

    Xu, Cheng-Qun; Li, Kui; Zhang, Wei-De

    2017-06-01

    Nitrogen-deficient graphitic carbon nitride (CN-HAc) was synthesized by thermal condensation of acetic acid-treated melamine as a precursor. The nitrogen vacancies play a remarkable role on controlling the electronic structure of g-C3N4, such as extending the optical absorption and enhancing the separation efficiency of photogenerated charge carriers, resulting in the improvement of photocatalytic activity. The photocatalytic activity of the catalysts was evaluated by splitting water and degradation of rhodamine B (RhB) under visible light irradiation (λ>420nm). The average H2 evolution rate on CN-HAc is 24μmolh(-1), which is about 5 times of that on pristine g-C3N4. Meanwhile, CN-HAc exhibits superior photocatalytic mineralization of RhB. The possible formation mechanism of nitrogen-deficient in the framework of g-C3N4 is proposed.

  7. Effect of thalidomide on tumour necrosis factor production and anti-tumour activity induced by 5,6-dimethylxanthenone-4-acetic acid.

    PubMed Central

    Ching, L. M.; Xu, Z. F.; Gummer, B. H.; Palmer, B. D.; Joseph, W. R.; Baguley, B. C.

    1995-01-01

    The investigational anti-tumour agent, 5,6-dimethylxanthenone-4-acetic acid (5,6-MeXAA), an analogue of flavone acetic acid (FAA), has been scheduled for clinical evaluation. Like FAA, 5,6-MeXAA exhibits excellent experimental anti-tumour activity and is an efficient inducer of cytokines in mice. We have examined the effect of pharmacological suppression of tumour necrosis factor (TNF) production on the anti-tumour activity of 5,6-MeXAA, taking advantage of previous observations that TNF production in response to endotoxin in vitro is inhibited by thalidomide. Thalidomide at doses of between 8 and 250 mg kg-1 efficiently suppressed serum TNF activity in response to 5,6-MeXAA at its optimal TNF inducing dose of 55 mg kg-1. Suppression was achieved when thalidomide was administered at the same time as, or up to 4 h before, 5,6-MeXAA. Under conditions in which TNF activity was suppressed, the degree of tumour haemorrhagic necrosis and the proportion of cures in the subcutaneous Colon 38 tumour were increased. In mice administered thalidomide (100 mg kg-1) together with 5,6-MeXAA (30 mg kg-1), complete tumour regression was obtained in 100% of mice, as compared with 67% in mice receiving 5,6-MeXAA alone. The results suggest a possible new application for thalidomide and pose new questions about the action of 5,6-MeXAA and related compounds. PMID:7640215

  8. A stability-indicating HPLC method for the determination of bazedoxifene acetate and its related substances in active pharmaceutical ingredient.

    PubMed

    Visweswara Rao, Karri; Reddy, Kesareddy Padmaja; Kumari, Kondapaturu Siva; Srinivas, Mudigonda

    2013-03-01

    A simple, cost effective, stability-indicating reversed-phase high-performance liquid chromatography method was developed for the quantitative determination of bazedoxifene acetate (BAZ) drug substance in the presence of its impurities and degradation products. The method was developed using an X-terra RP-18, 150 × 4.6 mm, 3.5 μm column with a mobile phase containing solvent A, a mixture of 10 mM K(2)HPO(4) (pH 8.3) and acetonitrile in the ratio of 70:30 (v/v); and solvent B, a mixture of water and acetonitrile in the ratio 10:90 (v/v). The eluted compounds were monitored at 220 nm, and within a short run time of 18 min, BAZ and its impurities were satisfactorily separated with resolution more than 2.0. BAZ was subjected to stress degradation and found to be sensitive towards acidic, basic, oxidative, thermal and hydrolytic stress conditions and stable in photo degradation conditions. The degradation products were well resolved from BAZ peak and its impurities; the mass balance in each case was more than 99.5%, proving the stability-indicating power of the method. The developed method was validated as per International Conference on Harmonization guidelines with respect to specificity, linearity (correlation coefficient > 0.9994), limit of detection, limit of quantification, accuracy (recovery range 96.3 to 102.1%), precision (relative standard deviation < 2.8%) and robustness.

  9. Evaluation of antioxidant and urease inhibition activities of roots of Glycyrrhiza glabra.

    PubMed

    Lateef, Mehreen; Iqbal, Lubna; Fatima, Nudrat; Siddiqui, Kauser; Afza, Nighat; Zia-ul-Haq, Muhammad; Ahmad, Mansoor

    2012-01-01

    The object of this study is to determine the antioxidant activity of extracts from Glycyrrhiza glabra roots. The parent extract is methanolic extract while its sub fractions were prepared in ethyl acetate, chloroform, and n-butanol. The method based on scavenging activity and reduction capability of 1, 1-diphenyl-2-picrylhydrazyl radical (DPPH). Urease inhibition activities of these extracts were also evaluated. Chloroform fraction was the most effective antioxidant with 87.7% activity but the activity is less than the crude methanolic extract i.e. 90%. Chloroform fraction showed the same trend in reducing power as that in radical scavenging activity. However n- butanol extract was devoid of any activity when compared to standard BHA. Crude methanolic fraction and its sub-fractions were also screened for enzyme inhibition activities using jackbean urease as substrate. Significant anti urease activity i.e. 72 % was observed in the ethyl acetate fraction with respect to standard inhibitor thiourea.

  10. Endophytic actinomycetes from spontaneous plants of Algerian Sahara: indole-3-acetic acid production and tomato plants growth promoting activity.

    PubMed

    Goudjal, Yacine; Toumatia, Omrane; Sabaou, Nasserdine; Barakate, Mustapha; Mathieu, Florence; Zitouni, Abdelghani

    2013-10-01

    Twenty-seven endophytic actinomycete strains were isolated from five spontaneous plants well adapted to the poor sandy soil and arid climatic conditions of the Algerian Sahara. Morphological and chemotaxonomical analysis indicated that twenty-two isolates belonged to the Streptomyces genus and the remaining five were non-Streptomyces. All endophytic strains were screened for their ability to produce indole-3-acetic acid (IAA) in vitro on a chemically defined medium. Eighteen strains were able to produce IAA and the maximum production occurred with the Streptomyces sp. PT2 strain. The IAA produced was further extracted, partially purified and confirmed by thin layer chromatography (TLC) analysis. The 16S rDNA sequence analysis and phylogenetic studies indicated that strain PT2 was closely related to Streptomyces enissocaecilis NRRL B 16365(T), Streptomyces rochei NBRC 12908(T) and Streptomyces plicatus NBRC 13071(T), with 99.52 % similarity. The production of IAA was affected by cultural conditions such as temperature, pH, incubation period and L-tryptophan concentration. The highest level of IAA production (127 μg/ml) was obtained by cultivating the Streptomyces sp. PT2 strain in yeast extract-tryptone broth supplemented with 5 mg L-tryptophan/ml at pH 7 and incubated on a rotary shaker (200 rpm) at 30 °C for 5 days. Twenty-four-hour treatment of tomato cv. Marmande seeds with the supernatant culture of Streptomyces sp. PT2 that contained the crude IAA showed the maximum effect in promoting seed germination and root elongation.

  11. Low potential detection of indole-3-acetic acid based on the peroxidase-like activity of hemin/reduced graphene oxide nanocomposite.

    PubMed

    Liu, Fengping; Tang, Jiaqian; Xu, Jun; Shu, Yun; Xu, Qin; Wang, Hongmei; Hu, Xiaoya

    2016-12-15

    An amperometric sensor was firstly established for the detection of indole-3-acetic acid (IAA) at low potential based on the hemin/reduced graphene oxide (hemin/rGO) composite. The hemin/rGO nanocomposite was prepared by a simple and facile hydrothermal method without using any reducing agent. It exhibited peroxidase-like activity for the catalytic oxidation of IAA in the presence of oxygen. The consumption of oxygen has a linear relationship with the concentration of IAA in the range from 0.1 to 43μM and from 43 to 183μM. The detection limit was down to 0.074μM. This sensor was unaffected by many interfering substances and stable over time. Such work broadened the application of hemin/rGO and provided a new method for IAA detection.

  12. Cytotoxicity and antimicrobial activity of marine macro algae (Dictyotaceae and Ulvaceae) from the Persian Gulf.

    PubMed

    Mashjoor, Sakineh; Yousefzadi, Morteza; Esmaeili, Mohamad Ali; Rafiee, Roya

    2016-10-01

    Pharmaceutical industry now accept the worlds ocean which contains a vast array of organisms with unique biological properties, as a major frontier for medical investigation. Bioactive compounds with different modes of action, such as, antiproliferative, antioxidant, antimicrotubule, have been isolated from marine sources, specifically macro and micro algae, and cyanobacteria. The aim of this work was to investigate antimicrobial and cytotoxic activities of the extracts of marine macro algae Ulva flexuosa, Padina antillarum and Padina boergeseni from the northern coasts of the Persian Gulf, Qeshm Island, Iran, against three cell lines including MCF7, HeLa and Vero, as well as their inhibitory effects against a wide array (i.e. n = 11) of pathogenic bacteria and fungi. Antimicrobial activity of the marine macro algal extracts was assessed using a disc diffusion method; an MTT cytotoxicity assay was employed to test the effects of the extracts on each cancer cell line. The algal extracts showed considerable antimicrobial activity against the majority of the tested bacteria and fungi. Both ethyl acetate and methanol extracts at the highest concentration (100 µg/ml) caused cell death, with the IC50 values calculated for each cell type and each algal extracts. Results are exhibited a higher decrease in the viability of the cells treated at the highest concentration of marine macro algal ethyl acetate extracts compared to the methanol extracts (78.9 % death in Vero cells by ethyl acetate extracts from U. flexuosa). Despite, the ethyl acetate extracts with lower dose- response of cells, exhibited better cytotoxic activity than methanol extracts (IC50: 55.26 μg/ml in Vero cells by ethyl acetate extracts from U. flexuosa). Based on the findings, it is concluded that the marine macro algal extracts from the Persian Gulf possess antibacterial and cytotoxic potential, which could be considered for future applications in medicine and identifying novel drugs from the

  13. Lead acetate does not inhibit dimethylnitrosamine activation and interacts with phenobarbital which is genotoxic in the ST cross of the Drosophila wing spot test.

    PubMed

    Castañeda-Partida, Laura; Heres-Pulido, Ma Eugenia; Guzmán-Rincón, Judith; Hernández-Portilla, Luis Barbo; Dueñas-García, Irma Elena; Durán-Díaz, Angel; Delfín-Alcalá, Irma

    2011-09-01

    Lead acetate (PbAc) is known to inhibit the synthesis of the heme group, needed for hemeproteins like Cytochromes P450 (CYP450s). Dimethylnitrosamine (DMN) requires metabolic activation by CYP450s. The Drosophila wing spot test was performed to establish whether PbAc inhibits DMN activation in the standard (ST) and high bioactivation (HB) crosses, with different levels of CYP450s. Phenobarbital (PH) was used as an antagonist for its ability to induce CYP450s synthesis. PbAc (0.01, 0.1, 1.0mM) produced significant small spots frequencies in the ST cross, indicating a possible genotoxic activity, however, the total spots frequency was negative at all concentrations. DMN (0.076 mM) was genotoxic in both crosses; surprisingly, PH (12 mM) was genotoxic and the PH-DMN treatment resulted synergic in the ST cross. Interestingly, the PbAc-PH pre-co-treatments showed a possible interaction in the ST cross. The GC-MS analysis showed a drop in the PH content as the PbAc concentration increased. PbAc also seemed to inhibit the genotoxic activity of PH, except at 0.01 mM. It is concluded that PbAc does not inhibit DMN activation by CYP450s in both crosses since it exerted a clear genotoxicity and that PH is genotoxic and interacts with PbAc in the ST but not the HB cross.

  14. Anticonvulsant and antinociceptive activity of new amides derived from 3-phenyl-2,5-dioxo-pyrrolidine-1-yl-acetic acid in mice.

    PubMed

    Rapacz, Anna; Obniska, Jolanta; Wiklik-Poudel, Beata; Rybka, Sabina; Sałat, Kinga; Filipek, Barbara

    2016-06-15

    The aim of the present experiments was to examine the anticonvulsant and antinociceptive activity of five new amides derived from 3-phenyl-2,5-dioxo-pyrrolidine-1-yl-acetic acid in animal models of seizures and pain. The antiseizure activity was investigated in three acute models of seizures, namely, the maximal electroshock (MES), the subcutaneous pentylenetetrazole (scPTZ), and 6Hz psychomotor seizure tests in mice. The antinociceptive properties were estimated in the formalin model of tonic pain, and in the oxaliplatin-induced neuropathic pain model in mice. Considering drug safety evaluation, acute neurological toxicity was determined in the rotarod test. Three tested compounds (3, 4, and 7) displayed a broad spectrum of anticonvulsant activity and showed better protective indices than those obtained for MES/scPTZ/6Hz active reference drug - valproic acid. Furthermore, three compounds (3, 4, and 6) demonstrated a significant antinociceptive effect in the formalin test, as well as antiallodynic activity in the oxaliplatin-induced neuropathic pain model. Among the tested agents, compounds 3 and 4 displayed not only antiseizure properties, but also collateral prominent analgesic properties. The in vitro binding study indicated that the plausible mechanism of action of chosen compound (4) was the influence on neuronal voltage-sensitive sodium (site 2) and L-type calcium channels.

  15. Furfuryl ethyl ether: important aging flavor and a new marker for the storage conditions of beer.

    PubMed

    Vanderhaegen, Bart; Neven, Hedwig; Daenen, Luk; Verstrepen, Kevin J; Verachtert, Hubert; Derdelinckx, Guy

    2004-03-24

    Recently, it was reported that furfuryl ethyl ether is an important flavor compound indicative of beer storage and aging conditions. A study of the reaction mechanism indicates that furfuryl ethyl ether is most likely formed by protonation of furfuryl alcohol or furfuryl acetate followed by S(N)2-substitution of the leaving group by the nucleophilic ethanol. For the reaction in beer, a pseudo-first-order reaction kinetics was derived. A close correlation was found between the values predicted by the kinetic model and the actual furfuryl ethyl ether concentration evolution during storage of beer. Furthermore, 10 commercial beers of different types, aged during 4 years in natural conditions, were analyzed, and it was found that the furfuryl ethyl ether flavor threshold was largely exceeded in each type of beer. In these natural aging conditions, lower pH, darker color, and higher alcohol content were factors that enhanced furfuryl ethyl ether formation. On the other hand, sulfite clearly reduced furfuryl ethyl ether formation. All results show that the furfuryl ethyl ether concentration is an excellent time-temperature integrator for beer storage.

  16. Preparation of vinyl acetate

    DOEpatents

    Tustin, Gerald Charles; Zoeller, Joseph Robert; Depew, Leslie Sharon

    1998-01-01

    This invention pertains to the preparation of vinyl acetate by contacting a mixture of hydrogen and ketene with a heterogeneous catalyst containing a transition metal to produce acetaldehyde, which is then reacted with ketene in the presence of an acid catalyst to produce vinyl acetate.

  17. Preparation of vinyl acetate

    DOEpatents

    Tustin, G.C.; Zoeller, J.R.; Depew, L.S.

    1998-03-24

    This invention pertains to the preparation of vinyl acetate by contacting a mixture of hydrogen and ketene with a heterogeneous catalyst containing a transition metal to produce acetaldehyde, which is then reacted with ketene in the presence of an acid catalyst to produce vinyl acetate.

  18. Lead acetate induces EGFR activation upstream of SFK and PKC{alpha} linkage to the Ras/Raf-1/ERK signaling

    SciTech Connect

    Wang, C.-Y.; Wang, Y.-T.; Tzeng, D.-W.; Yang, J.-L.

    2009-03-01

    Lead acetate (Pb), a probable human carcinogen, can activate protein kinase C (PKC) upstream of extracellular signal-regulated kinase 1 and 2 (ERK1/2). Yet, it remains unclear whether Pb activation of PKC {yields} ERK1/2 involves receptor/non-receptor tyrosine kinases and the Ras signaling transducer. Here we demonstrate a novel mechanism elicited by Pb for transmitting ERK1/2 signaling in CL3 human non-small-cell lung adenocarcinoma cells. Pb induction of higher steady-state levels of Ras-GTP was essential for increasing phospho-Raf-1{sup S338} and phospho-ERK1/2. Pre-treatment of the cells with a conventional PKC inhibitor Goe6976 or depleting PKC{alpha} using specific small interfering RNA blocked Pb induction of Ras-GTP. Pb also activated cellular tyrosine kinases. Specific pharmacological inhibitors, PD153035 for epidermal growth factor receptor (EGFR) and SU6656 for Src family tyrosine kinases (SFK), but not AG1296 for platelet-derived growth factor receptor, could suppress the Pb-induced tyrosine kinases, PKC{alpha}, Ras-GTP, phospho-Raf-1{sup S338} and phospho-ERK1/2. Furthermore, phosphorylation of tyrosines on the EGFR multiple autophosphorylation sites and the conserved SFK autophosphorylation site occurred during exposure of cells to Pb for 1-5 min and 5-30 min, respectively. Intriguingly, Pb activation of EGFR required the intrinsic kinase activity but not dimerization of the receptor. Inhibition of SFK or PKC{alpha} activities did not affect EGFR phosphorylation, while knockdown of EGFR blocked SFK phosphorylation and PKC{alpha} activation following Pb. Together, these results indicate that immediate activation of EGFR in response to Pb is obligatory for activation of SFK and PKC{alpha} and subsequent the Ras-Raf-1-MKK1/2-ERK1/2 signaling cascade.

  19. Residual behavior of quizalofop ethyl on onion (Allium cepa L.).

    PubMed

    Sahoo, S K; Mandal, Kousik; Singh, Gurmail; Kumar, Rajinder; Chahil, G S; Battu, R S; Singh, Balwinder

    2013-02-01

    Quizalofop ethyl, a phenoxy propionate herbicide, is used for postemergence control of annual and perennial grass weeds in broad-leaved crops in India. The experiments were designed to study the dissipation kinetics of quizalofop ethyl on onion for two seasons. A simple, rapid, and sensitive method for estimation of quizalofop ethyl residues in onion and soil was developed and validated. The recoveries of quizalofop ethyl residues from onion and soil at different spiking level range from 84.81 to 92.68 %. The limit of quantification of this method was found to be 0.01 μg g(-1). The risk assessment through consumption of the onion in comparison to its acceptable daily intake which is an important parameter for the safety of the consumer was also evaluated. Standardized methodology supported by recovery studies was adopted to estimate residues of quizalofop ethyl on onion and soil. The average initial deposits of quizalofop ethyl on onion were observed to be 0.25 and 0.33 mg kg(-1), following single application of the herbicide at 50 g active ingredient (a.i.) ha(-1) during 2009 and 2010, respectively. The half-life values (T (1/2)) of quizalofop ethyl on onion crop were worked out to be 0.85 and 0.79 days, respectively, during 2009 and 2010. At harvest time, the residues of quizalofop ethyl on onion and soil were found to be below the determination limit of 0.01 mg kg(-1) following single application of the herbicide at 50 and 100 g a.i. ha(-1) for both the periods.

  20. Assessment of the anti-angiogenic, anti-inflammatory and antinociceptive properties of ethyl vanillin.

    PubMed

    Jung, Hyun-Joo; Song, Yun Seon; Kim, Kyunghoon; Lim, Chang-Jin; Park, Eun-Hee

    2010-02-01

    The present work aimed to assess novel pharmacological properties of ethyl vanillin (EVA) which is used as a flavoring agent for cakes, dessert, confectionary, etc. EVA exhibited an inhibitory activity in the chorioallantoic membrane angiogenesis. Anti-inflammatory activity of EVA was convinced using the two in vivo models, such as vascular permeability and air pouch models in mice. Antinociceptive activity of EVA was assessed using acetic acid-induced writhing model in mice. EVA suppressed production of nitric oxide and induction of inducible nitric oxide synthase in the lipopolysaccharide (LPS)-activated RAW264.7 macrophage cells. However, EVA could not suppress induction of cyclooxygenase-2 in the LPS-activated macrophages. EVA diminished reactive oxygen species level in the LPS-activated macrophages. EVA also suppressed enhanced matrix metalloproteinase-9 gelatinolytic activity in the LPSactivated RAW264.7 macrophage cells. EVA at the used concentrations couldn't diminish viability of the macrophage cells. Taken together, the anti-angiogenic, anti-inflammatory and anti-nociceptive properties of EVA are based on its suppressive effect on the production of nitric oxide possibly via decreasing the reactive oxygen species level.

  1. Phorbol ester phorbol-12-myristate-13-acetate promotes anchorage-independent growth and survival of melanomas through MEK-independent activation of ERK1/2

    SciTech Connect

    Jorgensen, Kjersti; Skrede, Martina; Cruciani, Veronique; Mikalsen, Svein-Ole; Slipicevic, Ana; Florenes, Vivi Ann . E-mail: v.a.florenes@labmed.uio.no

    2005-04-01

    The phorbol ester, phorbol-12-myristate-13-acetate (PMA), an activator of PKCs, is known to stimulate the in vitro growth of monolayer cultures of normal human melanocytes whereas it inhibits the growth of most malignant melanoma cell lines. We examined the effect of PMA on proliferation and survival of melanoma cells grown as multicellular aggregates in suspension (spheroids), and aimed to elucidate downstream targets of PKC signaling. In contrast to monolayer cultures, PMA increased cell proliferation as well as protected melanoma cells from suspension-mediated apoptosis (anoikis). Supporting the importance of PKC in anchorage-independent growth, treatment of anoikis-resistant melanoma cell lines with antisense oligonucleotides against PKC-{alpha}, or the PKC inhibitor Goe6976, strongly induced anoikis. PMA induced activation of ERK1/2, but this effect was not prevented by the MEK inhibitors PD98059 or by U0126. Whereas PD98059 treatment alone led to marked activation of the pro-apoptotic Bim and Bad proteins and significantly increased anoikis, these effects were clearly reversed by PMA. In conclusion, our results indicate that the protective effect of PMA on anchorage-independent survival of melanoma cells at least partly is mediated by MEK-independent activation of ERK1/2 and inactivation of downstream pro-apoptotic effector proteins.

  2. Cloning, Purification and Characterization of Acetyl Xylane Esterase from Anoxybacillus flavithermus DSM 2641(T) with Activity on Low Molecular-Weight Acetates.

    PubMed

    Eminoğlu, Ayşenur; Ülker, Serdar; Sandallı, Cemal

    2015-08-01

    Family 4 carbohydrate esterases (CE-4) have deacetylate different forms of acetylated poly/oligosaccharides in nature. This family is recognized with a specific polysaccharide deacetylase domain assigned as NodB homology domain in their secondary structure. Most family 4 carbohydrate esterases have been structurally and biochemically characterized. However, this is the first study about the enzymological function of pdaB-like CE4s from thermophilic bacterium Anoxybacillus flavithermus DSM 2641(T). A. flavithermus WK1 genome harbors five putative CE4 family genes. One of them is 762 bp long and encodes a protein of 253 amino acids in length and it was used as reference sequence in this study. It was described as acetyl xylane esterase (AXE) in genome project and this AfAXE gene was amplified without signal sequence and cloned. The recombinant protein was expressed in E. coli BL21 (DE3), purified by nickel affinity chromatography and its purity was visualized on SDS-PAGE. The activity of the recombinant enzyme was shown by zymogram analysis with α-naphtyl acetate as a substrate. The enzyme was characterized spectrophotometrically using chromogenic p-nitrophenyl acetate. Optimum temperature and pH were determined as 50 °C and 7.5, respectively. Km and Vmax were determined as 0.43 mM and 3333.33 U/mg, respectively under optimum conditions. To our knowledge this is the first enzymological characterization of a pdaB-like family 4 carbohydrate esterase from the members of Anoxybacillus genus.

  3. Identification of phenolics in the fruit of emblica (Phyllanthus emblica L.) and their antioxidant activities.

    PubMed

    Liu, Xiaoli; Cui, Chun; Zhao, Mouming; Wang, Jinshui; Luo, Wei; Yang, Bao; Jiang, Yueming

    2008-08-15

    An activity-directed fractionation and purification process was used to identify the antioxidative components of emblica fruit. Dried fruit of emblica was extracted with methanol and then partitioned by ethyl ether, ethyl acetate, butanol and water. The ethyl acetate fraction showed the strongest 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity among four fractions. The ethyl acetate fraction was then subjected to separation and purification using Sephadex LH-20 chromatography and reverse-phase high-performance liquid chromatography (HPLC). Six compounds were identified to be geraniin (1), quercetin 3-β-d-glucopyranoside (2), kaempferol 3-β-d-glucopyranoside (3), isocorilagin (4), quercetin (5), and kaempferol (6), respectively, by spectral methods, (1)H and (13)C nuclear magnetic resonance (NMR) spectroscopy, ultraviolet-visible (UV-Vis) spectrophotometry and mass spectroscopy (MS), and comparison with literatures. Compounds 2-4 and 6 were identified from emblica fruit for the first time. Furthermore, the antioxidant activities of purified compounds were screened for their antioxidative potential using lipid peroxidation and DPPH systems. All the purified compounds showed strong antioxidant and radical scavenging activities. Amongst, geraniin showed the highest antioxidant activity (4.7 and 65.7μM of IC50 values for DPPH and lipid peroxidation assay, respectively) than other purified compounds.

  4. Efficacy of Angelica archangelica essential oil, phenyl ethyl alcohol and α- terpineol against isolated molds from walnut and their antiaflatoxigenic and antioxidant activity.

    PubMed

    Prakash, Bhanu; Singh, Priyanka; Goni, Reema; Raina, Ajay Kumar Pandit; Dubey, N K

    2015-04-01

    Mold association, aflatoxin B1 contamination as well as oxidative deterioration of agri-food items during storage and processing are some global task for food industries. In view of the adverse effects of some synthetic preservatives on treated food items and subsequently on consumers health, recently plant based chemicals are encouraged by food industries as better alternatives of synthetics. The present study recommends the combination (1:1:1) of Angelica archangelica essential oil: Phenyl ethyl alcohol (PEA): α- terpineol as botanical preservative against molds, aflatoxin contamination and oxidative deterioration of walnut samples. Eight mold species were procured from stored walnut samples, including some aflatoxigenic Aspergillus flavus strains. The combination inhibited growth of aflatoxigenic strain Aspergillus flavus NKDW-7 and aflatoxin B1 production at 2.25 and 2.0 μL mL(-1) respectively. The IC50 value of the combination was recorded as 3.89 μL mL(-1), showing strong antioxidant potential. The antifungal action of the combination showed > 90 % decrease in ergosterol content in plasma membrane of A. flavus at 2.0 μL mL(-1). The LD50 of the combination, through oral administration on mice, was 9562.9 μL kg(-1) body weight, indication favourable safety profile as a plant based preservative. The combination may be recommended as safe preservative against molds, aflatoxin contamination and oxidative deterioration of walnut samples.

  5. Synthesis, spectral characterization, thermal behaviour, antibacterial activity and DFT calculation on N‧-[bis(methylsulfanyl) methylene]-2-hydroxybenzohydrazide and N‧-(4-methoxy benzoyl)-hydrazinecarbodithioic acid ethyl ester

    NASA Astrophysics Data System (ADS)

    Bharty, M. K.; Dani, R. K.; Kushawaha, S. K.; Prakash, Om; Singh, Ranjan K.; Sharma, V. K.; Kharwar, R. N.; Singh, N. K.

    2015-06-01

    Two new compounds N‧-[bis(methylsulfanyl) methylene]-2-hydroxybenzohydrazide {Hbmshb (1)} and N‧-(4-methoxy benzoyl)-hydrazinecarbodithioic acid ethyl ester {H2mbhce (2)} have been synthesized and characterized with the aid of elemental analyses, IR, NMR and single crystal X-ray diffraction data. Compounds 1 and 2 crystallize in orthorhombic and monoclinic systems with space group Pna21 and P21/n, respectively. Inter and intra molecular hydrogen bonding link two molecules and provide linear chain structure. In addition to this, compound 2 is stabilized by CH⋯π and NH⋯π interactions. Molecular geometry from X-ray analysis, geometry optimization, charge distribution, bond analysis, frontier molecular orbital (FMO) analysis and non-linear optical (NLO) effects have been performed using the density functional theory (DFT) with the B3LYP functional. The bioefficacy of compounds has been examined against the growth of bacteria to evaluate their anti-microbial potential. Compounds 1 and 2 are thermally stable and show NLO behaviour better than the urea crystal.

  6. Cytotoxic Activity of Six Samples of Brazilian Propolis on Sea Urchin (Lytechinus variegatus) Eggs

    PubMed Central

    Fernandes-Silva, C. C.; Freitas, J. C.; Salatino, A.; Salatino, M. L. F.

    2013-01-01

    The cytotoxic activities of extracts of four samples of propolis from the state of Minas Gerais (Southeast Brazil) and two from the state of Paraná (South Brazil) were evaluated using sea urchin (Lytechinus variegatus) eggs. Cytotoxic activity was observed, characterized mainly by the inhibition of the first cleavage of newly fertilized eggs. Methanol extracts at 32 µg mL−1 of all samples were highly active (97–100%). Extracts were also prepared by successive treatments of the samples with hexane, chloroform, ethyl acetate, and methanol. High activity was observed using the ethyl acetate fractions of all samples, but hexane and chloroform fractions of some samples also had high activity. Based on the chemical composition of the extracts and fractions (published previously), it is hypothesized that the cytotoxic activities observed are due mainly to artepillin C, p-coumaric acid, and kaempferide. The results suggest that caffeoylquinic acids have no cytotoxic activity in sea urchin eggs. PMID:23662146

  7. Nitrosation Reactions of Ethyl Centralite

    DTIC Science & Technology

    1977-02-01

    up in ethyl alcohol, and the extract was treated with animai charcoal and filtered to give a yellow solution. Evaporation to half volume and dilution...stirrer, thermometer, and dropping funnel. Concentrated hydrochloric acid (25 ml) was slowly added while stirring, followed by a solution of a NaNO (6

  8. S-Ethyl dipropylthiocarbamate (EPTC)

    Integrated Risk Information System (IRIS)

    S - Ethyl dipropylthiocarbamate ( EPTC ) ; CASRN 759 - 94 - 4 Human health assessment information on a chemical substance is included in the IRIS database only after a comprehensive review of toxicity data , as outlined in the IRIS assessment development process . Sections I ( Health Hazard Assessme

  9. Detection of interstellar ethyl cyanide

    NASA Technical Reports Server (NTRS)

    Johnson, D. R.; Lovas, F. J.; Gottlieb, C. A.; Gottlieb, E. W.; Litvak, M. M.; Thaddeus, P.; Guelin, M.

    1977-01-01

    Twenty-four millimeter-wave emission lines of ethyl cyanide (CH3CH2CN) have been detected in the Orion Nebula (OMC-1) and seven in Sgr B2. To derive precise radial velocities from the astronomical data, a laboratory measurement of the rotational spectrum of ethyl cyanide has been made at frequencies above 41 GHz. In OMC-1, the rotational temperature of ethyl cyanide is 90 K (in good agreement with other molecules), the local-standard-of-rest radial velocity is 4.5 + or - 1.0 km/s (versus 8.5 km/s for most molecules), and the column density is 1.8 by 10 to the 14th power per sq cm (a surprisingly high figure for a complicated molecule). The high abundance of ethyl cyanide in the Orion Nebula suggests that ethane and perhaps larger saturated hydrocarbons may be common constituents of molecular clouds and have escaped detection only because they are nonpolar or only weakly polar.

  10. Synthesis, Spectral Characterization, In-vitro Antibacterial and Antifungal Activities of Novel (2e)-Ethyl-2-(2-(2, 4-Dinitrophenyl) Hydrazono)-4-(Naphthalen-2-yl)-6-Arylcyclohex-3-Enecarboxylates

    PubMed Central

    Kanagarajan, V; Thanusu, J; Gopalakrishnan, M

    2011-01-01

    In a search for new leads towards potent antimicrobial agents, an array of novel (2E)-ethyl-2-(2-(2,4-dinitrophenyl)hydrazono)-4-(naphthalen-2-yl)-6-arylcyclohex-3-ene carboxylates 17-24 were synthesized and characterized through their melting point, elemental analysis, MS, FT-IR, one-dimensional NMR (1H, D2O exchanged 1H and 13C), two dimensional HOMOCOR and HSQC spectroscopic data. In-vitro microbiological evaluations were carried out for all the newly synthesized compounds 17-24 against clinically isolated bacterial strains namely Salmonella typhii, Klebsiellapneumoniae, Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, β-Hemolytic streptococcus and Micrococcus luteusand also fungal strains namely Aspergillusflavus, Aspergillusniger, Mucor, Rhizopus and Microsporumgypseumand finally, the results of their structure activity relationship were discussed. The obtained results can be used as the key step for the building of novel chemical compounds with interesting antimicrobial profiles comparable to that of the standard drugs. PMID:24250406

  11. Effects of Sequential Applications of Bassa 50EC (Fenobucarb) and Vitashield 40EC (Chlorpyrifos ethyl) on Acetylcholinesterase Activity in Climbing Perch (Anabas testudineus) Cultured in Rice Fields in the Mekong Delta, Vietnam.

    PubMed

    Tam, Nguyen Thanh; Berg, Håkan; Laureus, Jenny; Cong, Nguyen Van; Tedengren, Michael

    2016-07-01

    This study assesses the effects of sequential applications of the insecticides Bassa 50EC (fenobucarb-F) and Vitashield 40EC (chlorpyrifos ethyl-CPF), sprayed at concentrations used by rice farmers in the Mekong Delta, on the brain acetylcholinesterase (AChE) in climbing perch fingerlings. After spraying the pesticides on the rice fields, the water concentrations of both insecticides decreased below the detection levels within 3 days. The sequential applications caused significant inhibition on the brain AChE activity in the exposed fish. The inhibition by F was quicker, but less prolonged, than for CPF. The inhibition levels caused by the sequential applications were lower than those caused by only CPF and by a mixture of CPF and F. The results indicate that sequential applications of pesticides could have a negative impact on aquatic organisms and fish yields, with implication for the aquatic biodiversity, local people's livelihood and the aquaculture industry in the Mekong Delta.

  12. Nanofabrication in cellulose acetate.

    PubMed

    Zeng, Hongjun; Lajos, Robert; Metlushko, Vitali; Elzy, Ed; An, Se Young; Sautner, Joshua

    2009-03-07

    We have demonstrated nanofabrication with commercialized cellulose acetate. Cellulose acetate is used for bulk nanofabrication and surface nanofabrication. In bulk nanofabrication, cellulose acetate reacts with an e-beam and permanent patterns are formed in it instead of being transferred to other substrates. We have studied the nano relief modulation performance of cellulose acetate before and after development. The depth of the nanopatterns is magnified after development, and is varied by exposing dosage and line width of the pattern. The thinnest 65 nm wide line is achieved in the bulk fabrication. We also demonstrate a binary phase Fresnel lens array which is directly patterned in a cellulose acetate sheet. Because of its unique mechanical and optical properties, cellulose is a good candidate for a template material for soft imprinting lithography. In the surface nanofabrication, cellulose acetate thin film spin-coated on silicon wafers is employed as a new resist for e-beam lithography. We achieved 50 nm lines with 100 nm pitches, dots 50 nm in diameter, and single lines with the smallest width of 20 nm. As a new resist of e-beam lithography, cellulose acetate has high resolution comparable with conventional resists, while having several advantages such as low cost, long stock time and less harmfulness to human health.

  13. Oxidation of ethyl ether on borate glass: chemiluminescence, mechanism, and development of a sensitive gas sensor.

    PubMed

    Hu, Jing; Xu, Kailai; Jia, Yunzhen; Lv, Yi; Li, Yubao; Hou, Xiandeng

    2008-11-01

    A gas sensor was developed by using the chemiluminescence (CL) emission from the oxidation of ethyl ether by oxygen in the air on the surface of borate glass. Theoretical calculation, together with experimental investigation, revealed the main CL reactions: ethyl ether is first oxidized to acetaldehyde and then to acetic acid, during which main luminous intermediates such as CH 3CO (*) are generated and emit light with a peak at 493 nm. At a reaction temperature of 245 degrees C, the overall maximal emission was found at around 460 nm, and the linear range of the CL intensity versus the concentration of ethyl ether was 0.12-51.7 microg mL (-1) ( R = 0.999, n = 7) with a limit of detection (3sigma) of 0.04 microg mL (-1). Interference from foreign substances including alcohol (methanol, ethanol and isopropanol), acetone, ethyl acetate, n-hexane, cyclohexane, dichloromethane, or ether ( n-butyl ether, tetrahydrofuran, propylene oxide, isopropyl ether and methyl tert-butyl ether) was not significant except a minimal signal from n-butyl ether (<2%). It is a simple, sensitive and selective gas sensor for the determination of trace ethyl ether.

  14. Synthesis and in Vitro Antifungal Activity against Botrytis cinerea of Geranylated Phenols and Their Phenyl Acetate Derivatives

    PubMed Central

    Chávez, María I.; Soto, Mauricio; Taborga, Lautaro; Díaz, Katy; Olea, Andrés F.; Bay, Camila; Peña-Cortés, Hugo; Espinoza, Luis

    2015-01-01

    The inhibitory effects on the mycelial growth of plant pathogen Botritys cinerea have been evaluated for a series of geranylphenols substituted with one, two and three methoxy groups in the aromatic ring. The results show that the antifungal activity depends on the structure of the geranylphenols, increasing from 40% to 90% by increasing the number of methoxy groups. On the other hand, the acetylation of the –OH group induces a change of activity that depends on the number of methoxy groups. The biological activity of digeranyl derivatives is lower than that exhibited by the respective monogeranyl compound. All tested geranylphenols have been synthesized by direct coupling of geraniol and the respective phenol. The effect of solvent on yields and product distribution is discussed. For monomethoxyphenols the reaction gives better yields when acetonitrile is used as a solvent and AgNO3 is used as a secondary catalyst. However, for di- and trimethoxyphenols the reaction proceeds only in dioxane. PMID:26287171

  15. Synthesis and in Vitro Antifungal Activity against Botrytis cinerea of Geranylated Phenols and Their Phenyl Acetate Derivatives.

    PubMed

    Chávez, María I; Soto, Mauricio; Taborga, Lautaro; Díaz, Katy; Olea, Andrés F; Bay, Camila; Peña-Cortés, Hugo; Espinoza, Luis

    2015-08-14

    The inhibitory effects on the mycelial growth of plant pathogen Botritys cinerea have been evaluated for a series of geranylphenols substituted with one, two and three methoxy groups in the aromatic ring. The results show that the antifungal activity depends on the structure of the geranylphenols, increasing from 40% to 90% by increasing the number of methoxy groups. On the other hand, the acetylation of the -OH group induces a change of activity that depends on the number of methoxy groups. The biological activity of digeranyl derivatives is lower than that exhibited by the respective monogeranyl compound. All tested geranylphenols have been synthesized by direct coupling of geraniol and the respective phenol. The effect of solvent on yields and product distribution is discussed. For monomethoxyphenols the reaction gives better yields when acetonitrile is used as a solvent and AgNO3 is used as a secondary catalyst. However, for di- and trimethoxyphenols the reaction proceeds only in dioxane.

  16. Cell-type-specific activity of the human papillomavirus type 18 upstream regulatory region in transgenic mice and its modulation by tetradecanoyl phorbol acetate and glucocorticoids.

    PubMed Central

    Cid, A; Auewarakul, P; Garcia-Carranca, A; Ovseiovich, R; Gaissert, H; Gissmann, L

    1993-01-01

    The upstream regulatory region (URR) of human papillomavirus type 18 (HPV-18) harbors transcriptional promoter and enhancer elements which are thought to determine the cell-type specificity of the virus. In order to study the regulation of HPV-18 expression in vivo, we constructed transgenic mice carrying the bacterial lacZ gene under the control of the HPV-18 URR. Analysis of beta-galactosidase activity by histochemical staining of tissue sections of four independent transgenic mice showed that the viral promoter was specifically active in epithelial cells within a variety of organs (e.g., tongue, ovary, uterus, testis, and small intestine). Very strong staining was observed in newborn transgenic mice in contrast to a weak activity found during fetal life. Determination of beta-galactosidase activity in crude extracts from tissues of three lines of transgenic mice proved to be a useful tool for a quantitative analysis of transgene expression. In mice from two different transgenic lines treated with dexamethasone such measurements revealed a biphasic effect of the hormone on the activity of the enzyme in the stratified epithelium of the tongue (transient increase followed by a decrease). Northern (RNA) blot analysis showed similar changes in beta-galactosidase mRNA in that tissue. Treatment with tetradecanoyl phorbol acetate (TPA) led to a twofold increase in both enzymatic activity and mRNA levels. Finally, combined treatments with dexamethasone and TPA showed that both factors interfered with each other in their respective effects on transgene expression, suggesting that a cross-talk mechanism between transcription factors could be involved in the regulation of the HPV-18 URR. Images PMID:8411377

  17. Aryl-acetic and cinnamic acids as lipoxygenase inhibitors with antioxidant, anti-inflammatory, and anticancer activity.

    PubMed

    Hadjipavlou-Litina, Dimitra; Pontiki, Eleni

    2015-01-01

    Cinnamic acids have been identified as interesting compounds with cytotoxic, anti-inflammatory, and antioxidant properties. Lipoxygenase pathway, catalyzing the first two steps of the transformation of arachidonic acid into leukotrienes is implicated in several processes such as cell differentiation, inflammation and carcinogenesis. Development of drugs that interfere with the formation or effects of these metabolites would be important for the treatment of various diseases like asthma, psoriasis, ulcerative colitis, rheumatoid arthritis, atherosclerosis, cancer, and blood vessel disorders. Till now, asthma consists of the only pathological case in which improvement has been shown by lipoxygenase LO inhibitors. Thus, the research has been directed towards the development of drugs that interfere with the formation of leukotrienes. In order to explore the anti-inflammatory and cytotoxic effects of antioxidant acrylic/cinnamic acids a series of derivatives bearing the appropriate moieties have been synthesized via the Knoevenagel condensation and evaluated for their biological activities. The compounds have shown important antioxidant activity, anti-inflammatory activity and very good inhibition of soybean lipoxygenase while some of them were tested for their anticancer activity.

  18. Analgesic, antibacterial and central nervous system depressant activities of Albizia procera leaves

    PubMed Central

    Khatoon, Mst. Mahfuza; Khatun, Mst. Hajera; Islam, Md. Ekramul; Parvin, Mst. Shahnaj

    2014-01-01

    Objective To ascertain analgesic, antibacterial and central nervous system (CNS) depressant activities of ethyl acetate, dichloromethane and carbon tetrachloride fractions of methanol extract of Albizia procera (A. procera) leaves. Methods Leaves extracts of A. procera were tested for analgesic activity by acetic acid induced and formalin test method in mice. The in vitro antibacterial activity was performed by agar well diffusion method. CNS depressant activity was evaluated by hole cross and open field tests. Results All the extracts at 200 mg/kg exhibited significant (P<0.01) analgesic activity in acetic acid induced and formalin tests method in mice. Analgesic activity of the ethyl acetate fraction was almost same like as standard drug indomethacin in acetic acid induced method. The CNS depressant activity of the extracts at 500 mg/kg was comparable to the positive control diazepam as determined by hole cross and open field test method. The extracts exhibited moderate antimicrobial activity against all the tested microorganisms (Staphylococcus aureus, Bacillus cereus, Pseudomonas aeruginosa, Esherichia coli, Shigella soneii, Shigella boydii) at concentration of 0.8 mg/disc. The measured diameter of zone of inhibition for the extracts was within the range of 7 to 12 mm which was less than the standard kanamycin (16-24 mm). Conclusions It is concluded that all the extracts possess potential analgesic and CNS depressants activity. This study also showed that different fractions of methanol extract could be potential sources of new antimicrobial agents. PMID:25182551

  19. 49 CFR 173.322 - Ethyl chloride.

    Code of Federal Regulations, 2012 CFR

    2012-10-01

    ... 49 Transportation 2 2012-10-01 2012-10-01 false Ethyl chloride. 173.322 Section 173.322 Transportation Other Regulations Relating to Transportation PIPELINE AND HAZARDOUS MATERIALS SAFETY... SHIPMENTS AND PACKAGINGS Gases; Preparation and Packaging § 173.322 Ethyl chloride. Ethyl chloride must...

  20. 49 CFR 173.322 - Ethyl chloride.

    Code of Federal Regulations, 2013 CFR

    2013-10-01

    ... 49 Transportation 2 2013-10-01 2013-10-01 false Ethyl chloride. 173.322 Section 173.322 Transportation Other Regulations Relating to Transportation PIPELINE AND HAZARDOUS MATERIALS SAFETY... SHIPMENTS AND PACKAGINGS Gases; Preparation and Packaging § 173.322 Ethyl chloride. Ethyl chloride must...

  1. 49 CFR 173.322 - Ethyl chloride.

    Code of Federal Regulations, 2014 CFR

    2014-10-01

    ... 49 Transportation 2 2014-10-01 2014-10-01 false Ethyl chloride. 173.322 Section 173.322 Transportation Other Regulations Relating to Transportation PIPELINE AND HAZARDOUS MATERIALS SAFETY... SHIPMENTS AND PACKAGINGS Gases; Preparation and Packaging § 173.322 Ethyl chloride. Ethyl chloride must...

  2. 49 CFR 173.322 - Ethyl chloride.

    Code of Federal Regulations, 2010 CFR

    2010-10-01

    ... 49 Transportation 2 2010-10-01 2010-10-01 false Ethyl chloride. 173.322 Section 173.322 Transportation Other Regulations Relating to Transportation PIPELINE AND HAZARDOUS MATERIALS SAFETY... SHIPMENTS AND PACKAGINGS Gases; Preparation and Packaging § 173.322 Ethyl chloride. Ethyl chloride must...

  3. 21 CFR 172.868 - Ethyl cellulose.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 3 2011-04-01 2011-04-01 false Ethyl cellulose. 172.868 Section 172.868 Food and... Multipurpose Additives § 172.868 Ethyl cellulose. The food additive ethyl cellulose may be safely used in food in accordance with the following prescribed conditions: (a) The food additive is a cellulose...

  4. 21 CFR 172.868 - Ethyl cellulose.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 3 2012-04-01 2012-04-01 false Ethyl cellulose. 172.868 Section 172.868 Food and... Multipurpose Additives § 172.868 Ethyl cellulose. The food additive ethyl cellulose may be safely used in food in accordance with the following prescribed conditions: (a) The food additive is a cellulose...

  5. 21 CFR 172.868 - Ethyl cellulose.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 3 2013-04-01 2013-04-01 false Ethyl cellulose. 172.868 Section 172.868 Food and... Multipurpose Additives § 172.868 Ethyl cellulose. The food additive ethyl cellulose may be safely used in food in accordance with the following prescribed conditions: (a) The food additive is a cellulose...

  6. 21 CFR 573.420 - Ethyl cellulose.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Ethyl cellulose. 573.420 Section 573.420 Food and... Listing § 573.420 Ethyl cellulose. The food additive ethyl cellulose may be safely used in animal feed in accordance with the following prescribed conditions: (a) The food additive is a cellulose ether...

  7. 21 CFR 172.868 - Ethyl cellulose.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 3 2010-04-01 2009-04-01 true Ethyl cellulose. 172.868 Section 172.868 Food and... Multipurpose Additives § 172.868 Ethyl cellulose. The food additive ethyl cellulose may be safely used in food in accordance with the following prescribed conditions: (a) The food additive is a cellulose...

  8. 21 CFR 184.1293 - Ethyl alcohol.

    Code of Federal Regulations, 2011 CFR

    2011-04-01

    ... 21 Food and Drugs 3 2011-04-01 2011-04-01 false Ethyl alcohol. 184.1293 Section 184.1293 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) FOOD FOR HUMAN... Substances Affirmed as GRAS § 184.1293 Ethyl alcohol. (a) Ethyl alcohol (ethanol) is the chemical C2H5OH....

  9. 21 CFR 184.1293 - Ethyl alcohol.

    Code of Federal Regulations, 2013 CFR

    2013-04-01

    ... 21 Food and Drugs 3 2013-04-01 2013-04-01 false Ethyl alcohol. 184.1293 Section 184.1293 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) FOOD FOR HUMAN... Substances Affirmed as GRAS § 184.1293 Ethyl alcohol. (a) Ethyl alcohol (ethanol) is the chemical C2H5OH....

  10. 21 CFR 184.1293 - Ethyl alcohol.

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 21 Food and Drugs 3 2014-04-01 2014-04-01 false Ethyl alcohol. 184.1293 Section 184.1293 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) DIRECT FOOD....1293 Ethyl alcohol. (a) Ethyl alcohol (ethanol) is the chemical C2H5OH. (b) The ingredient meets...

  11. 21 CFR 184.1293 - Ethyl alcohol.

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 21 Food and Drugs 3 2010-04-01 2009-04-01 true Ethyl alcohol. 184.1293 Section 184.1293 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) FOOD FOR HUMAN... Substances Affirmed as GRAS § 184.1293 Ethyl alcohol. (a) Ethyl alcohol (ethanol) is the chemical C2H5OH....

  12. 21 CFR 184.1293 - Ethyl alcohol.

    Code of Federal Regulations, 2012 CFR

    2012-04-01

    ... 21 Food and Drugs 3 2012-04-01 2012-04-01 false Ethyl alcohol. 184.1293 Section 184.1293 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) FOOD FOR HUMAN... Substances Affirmed as GRAS § 184.1293 Ethyl alcohol. (a) Ethyl alcohol (ethanol) is the chemical C2H5OH....

  13. Inhibitory effect of herbal remedies on 12-O-tetradecanoylphorbol-13-acetate-promoted Epstein-Barr virus early antigen activation.

    PubMed

    Kapadia, Govind J; Azuine, Magnus A; Tokuda, Harukuni; Hang, Eric; Mukainaka, T; Nishino, Hoyoku; Sridhar, Rajagopalan

    2002-03-01

    For the past several years we have been evaluating natural products as potential cancer chemopreventive agents in a short term in vitro assay involving Epstein--Barr virus early antigen (EBV-EA) activation in Raji cells promoted by phorbol ester, 12-O-tetradecanoylphorbol-13-acetate (TPA). Because of the current interest in the use of herbal remedies, we considered examining them for their cancer chemopreventive activities, using their extracts with a view to uncovering such benefits (if any) these remedies might possess. Thirty-six extracts of 32 herbs belonging to 27 families in use as herbal remedies including those of gingko, black cohosh, echinacea, kava-kava, saw palmetto, turmeric, angelica, wild yam, cat's claw, passion flower, muira puama, feverfew, blueberry, chasteberry, licorice, nettle, golden seal, pygeum, ginger, valerian and hops were prepared and evaluated. Turmeric at a concentration of 10 microg x ml (-1)exhibited the most potent anti-EBV-EA activity, which is ten times more than passionflower, that is next in the order of activity. At the concentration level of 100 microg ml (-1), several of the herbal remedies tested inhibited the EBV-EA in Raji cells exposed to the tumor promoter TPA (32 pM) by more than 90%. We also report for the first time the activities of 16 new medicinal plants as potential cancer chemopreventive agents. Since inhibitors of EBV-EA promoted by TPA in vitro have been shown to be effective anti-tumor promoting agents in laboratory animal models, our results indicate new and potential applications of these herbal remedies as cancer chemopreventive agents since they are already in clinical use in the human population.

  14. Antiproliferative activity, cell-cycle dysregulation, and cellular differentiation: salicyl- and catechol-derived acyclic 5-fluorouracil O,N-acetals against breast cancer cells.

    PubMed

    Marchal, Juan A; Rodríguez-Serrano, Fernando; Caba, Octavio; Aránega, Antonia; Gallo, Miguel A; Espinosa, Antonio; Campos, Joaquín M

    2007-12-01

    Herein we report the preparation and biological activity of three compounds with the general formula 1-[2-(5-substituted-2-hydroxybenzyloxy)-1-methoxyethyl]-5-fluorouracil. A catechol-derived compound such as 1-[3-(2-hydroxyphenoxy)-1-methoxypropyl]-5-fluorouracil and two salicyl-derived compounds such as (Z)-1-[4-(2-hydroxyphenyl)-1-methoxybut-3-enyl]-5-fluorouracil [(Z)-11] and its dihydrogenated derivative 1-[4-(2-hydroxyphenyl)-1-methoxybutyl]-5-fluorouracil were prepared to complete the set of six O,N-acetals. The most active compound against the MCF-7 breast cancer cell line was (Z)-11: IC(50)=9.40+/-0.64 microM. Differentiated breast cancer cells generate fat deposits in the cytoplasm. MCF-7 cells treated with (Z)-11 underwent an increase in lipid content relative to control cells after three days of treatment. Our results suggest that there may be significant potential advantages in the use of this new differentiating agent for the treatment of breast cancer.

  15. Effect of surface modification of an engineered activated carbon on the sorption of 2,4-dichlorophenoxy acetic acid and benazolin from water.

    PubMed

    Chingombe, P; Saha, B; Wakeman, R J

    2006-05-15

    The performance of a conventional (F400) and a surface modified activated carbon (F400AN) has been investigated for the sorption of benazolin and 2,4-dichlorophenoxy acetic acid (2,4-D) from water. It was observed that the modified carbon, F400AN, which was obtained by annealing the conventional sample had a higher BET surface area (960 m2 g(-1) compared to 790 m2 g(-1)) and it had a higher proportion of micropores. This was attributed to the loss of oxygen containing functional groups during the thermal treatment. Zeta potential and pH titration measurements also showed that acidic functionality had been lost on the F400AN sample. The adsorption data were analysed and were fitted well using the Langmuir isotherm. The modified carbon marginally out-performed the conventional activated carbon for sorption of these two herbicides. Thermodynamic parameters (DeltaG0, DeltaH0, and DeltaS0) were determined and their values indicated that the sorption process was spontaneous and endothermic for both herbicides. A pseudo-second-order kinetic model was employed for analysing the kinetic data. It was concluded that the herbicide sorption process was controlled by a film diffusion mechanism.

  16. Antimycobacterial and Nitric Oxide Production Inhibitory Activities of Ocotea notata from Brazilian Restinga

    PubMed Central

    Costa, Isabela Francisca Borges; Calixto, Sanderson Dias; Heggdorne de Araujo, Marlon; Konno, Tatiana Ungaretti Paleo; Tinoco, Luzineide Wanderley; Guimarães, Denise Oliveira; Lasunskaia, Elena B.; Leal, Ivana Ramos Correa; Muzitano, Michelle Frazão

    2015-01-01

    The genus Ocotea (Lauraceae) is distributed mainly in tropical and subtropical regions. Some species of this genus as O. puberula and O. quixos have been described in the literature, showing antibacterial activity. And Ocotea macrophylla showed anti-inflammatory activity with inhibition of COX-1, COX-2, and LOX-5. The purpose of this study was the phytochemical investigation of the plant species Ocotea notata from Restinga Jurubatiba National Park, Macaé, RJ, Brazil, and the search for antimycobacterial fractions and compounds. The crude extract was evaluated for antimycobacterial activity and presented 95.75 ± 2.53% of growth inhibition at 100 µg/mL. Then, it was subjected to a liquid-liquid partition and subsequently was chemically investigated by HPLC, revealing the major presence of flavonoids. In this process the partition fractions hexane, ethyl acetate, and butanol are shown to be promising in the antimycobacterial assay. In addition, ethyl acetate fraction was chromatographed and afforded two flavonoids identified by MS and NMR as afzelin and isoquercitrin. The isolated flavonoids afzelin and isoquercitrin were evaluated for their antimycobacterial activity and for their ability to inhibit NO production by macrophages stimulated by LPS; both flavonoids isoquercitrin (Acet22) and afzelin (Acet32) were able to inhibit the production of NO by macrophages. The calculated IC50 of Acet22 and Acet32 was 1.03 and 0.85 µg/mL, respectively. PMID:25789338

  17. Nasal pungency, odor, and eye irritation thresholds for homologous acetates.

    PubMed

    Cometto-Muñiz, J E; Cain, W S

    1991-08-01

    We measured detection thresholds for nasal pungency (in anosmics), odor (in normosmics) and eye irritation employing a homologous series of acetates: methyl through octyl acetate, decyl and dodecyl acetate. All anosmics reliably detected the series up to heptyl acetate. Only the anosmics without smell since birth (congenital) reliably detected octyl acetate, and only one congenital anosmic detected decyl and dodecyl acetate. Anosmics who lost smell from head trauma proved to be selectively less sensitive. As expected, odor thresholds lay well below pungency thresholds. Eye irritation thresholds for selected acetates came close to nasal pungency thresholds. All three types of thresholds decreased logarithmically with carbon chain length, as previously seen with homologous alcohols and as seen in narcotic and toxic phenomena. Results imply that nasal pungency for these stimuli rests upon a physical, rather than chemical, interaction with susceptible mucosal structures. When expressed as thermodynamic activity, nasal pungency thresholds remain remarkably constant within and across the homologous series of acetates and alcohols.

  18. Bioefficacy of Alpinia galanga (Zingiberaceae) rhizome extracts, (E)-p-acetoxycinnamyl alcohol, and (E)-p-coumaryl alcohol ethyl ether against Bactrocera dorsalis (Diptera: Tephritidae) and the impact on detoxification enzyme activities.

    PubMed

    Sukhirun, N; Pluempanupat, W; Bullangpoti, V; Koul, O

    2011-10-01

    The application of insecticides to control oriental fruit fly, Bactrocera dorsalis Hendel (Diptera: Tephritidae), is a principal component of the current management of these fruit flies. However, we evaluated four extracts of Alpinia galanga Wild Linn (Zingiberaceae) rhizomes against adult flies and found hexane and ethanol extracts to be most effective (LC50 = 4,866 and 6,337 ppm, respectively, after 24 h). This suggested that both nonpolar and polar compounds could be active in the candidate plant. Accordingly, the hexane extract was further processed to isolate nonpolar active compounds from this plant source. Two compounds, (E)-p-acetoxycinnamyl alcohol and (E)-p-coumaryl alcohol ethyl ether, were identified as active ingredients and found to be more active than total hexane extract (LC50 = 3,654 and 4,044 ppm, respectively, after 24 h). The data suggested that the compounds were not synergistic but may have some additive effect in a mixture. The activity of the hexane extract against detoxification enzymes, carboxylesterase (CE) and glutathione transferase (GST) also was determined in vitro. CE was inhibited by 70%, whereas GST was not significantly inhibited. Insect CEs mediate insecticide resistance via their induction; therefore, inhibition of these enzymes by plant allelochemicals could be a useful alternative approach for the management of the pest in the field.

  19. Ethyl Pyruvate Combats Human Leukemia Cells but Spares Normal Blood Cells

    PubMed Central

    Kurz, Susanne; Bigl, Marina; Buchold, Martin; Thieme, Rene; Wichmann, Gunnar; Dehghani, Faramarz

    2016-01-01

    Ethyl pyruvate, a known ROS scavenger and anti-inflammatory drug was found to combat leukemia cells. Tumor cell killing was achieved by concerted action of necrosis/apoptosis induction, ATP depletion, and inhibition of glycolytic and para-glycolytic enzymes. Ethyl lactate was less harmful to leukemia cells but was found to arrest cell cycle in the G0/G1 phase. Both, ethyl pyruvate and ethyl lactate were identified as new inhibitors of GSK-3β. Despite the strong effect of ethyl pyruvate on leukemia cells, human cognate blood cells were only marginally affected. The data were compiled by immune blotting, flow cytometry, enzyme activity assay and gene array analysis. Our results inform new mechanisms of ethyl pyruvate-induced cell death, offering thereby a new treatment regime with a high therapeutic window for leukemic tumors. PMID:27579985

  20. Optimization in the formaldehyde determination at sub-ppm level from acetals by HPLC-DAD

    SciTech Connect

    Medvedovici, A.; David, V.; David, F.; Sandra, P.

    1999-02-01

    Carbonylic compounds are mainly monitored as atmospheric pollutants, due to their major contribution to the formation of free radicals and ozone, by means of photolysis. Determination of formaldehyde at sub-ppm level as impurity in acetals using HPLC-DAD is described. Automated on-line precolumn derivatization reaction with 2,4-dinitrophenylhydrazine has been used. Breakdown rates of some industrial scale used acetals (Methylal, Ethylal) to formaldehyde by hydrolysis in aqueous media, according to pH, are described.

  1. Coumarins and flavonoid from Murraya paniculata (L.) Jack: Antibacterial and anti-inflammation activity.

    PubMed

    Rodanant, Pirasut; Khetkam, Pichit; Suksamrarn, Apichart; Kuvatanasuchati, Jintakorn

    2015-11-01

    The ethyl acetate extract of leaves of Murraya paniculata (L.) Jack was described in the previous in vitro study on the inhibition effect on the growth of periodontopathic bacteria and the reduction of cytokines from LPS-stimulated macrophages. In this study, four coumarins including murrangatin (1), murrangatin acetate (2), murranganonesenecionate (3), micropubescin (4) and one flavonoid, 3', 4', 5', 7-tetramethoxyflavone (5) were isolated from the leaves of ethyl acetate extract of M. paniculata. MTT assay was used to test cytotoxicity on human gingival fibroblast and monocytes. The isolated compounds were evaluated for their antibacterial effect against Porphyromonas gingivalis (ATCC33277) and anti-inflammation on lipopolysaccharide-stimulated inflammation using monocyte cells. All isolated compounds exhibited antibacterial activity against P. gingivalis (ATCC 33277). Murranganonesenecionate (3) was highly potent anti-inflammation properties. The coumarin constituents from M. paniculata leaves might be potential lead molecules for the development of antimicrobial drugs for treating periodontal disease.

  2. Evaluation of the antioxidant activity of Syzygium cumini leaves.

    PubMed

    Ruan, Zhi Ping; Zhang, Liang Liang; Lin, Yi Ming

    2008-01-01

    The antioxidant activity of Syzygium cumini leaf extracts was investigated using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical-scavenging and ferric-reducing antioxidant power (FRAP) assays. The methanolic extract and its four water, ethyl acetate, chloroform, and n-hexane fractions were prepared and subjected to antioxidant evaluation. The results showed that the ethyl acetate fraction had stronger antioxidant activity than the other ones. HPLC data indicated that S. cumini leaf extracts contained phenolic compounds, such as ferulic acid and catechin, responsible for their antioxidant activity. A significant linear relationship between antioxidant potency, free radical-scavenging ability and the content of phenolic compounds of leaf extracts supported this observation.

  3. Acetate ester production by Chinese yellow rice wine yeast overexpressing the alcohol acetyltransferase-encoding gene ATF2.

    PubMed

    Zhang, J; Zhang, C; Qi, Y; Dai, L; Ma, H; Guo, X; Xiao, D

    2014-11-27

    Acetate ester, which are produced by fermenting yeast cells in an enzyme-catalyzed intracellular reaction, are responsible for the fruity character of fermented alcoholic beverages such as Chinese yellow rice wine. Alcohol acetyltransferase (AATase) is currently believed to be the key enzyme responsible for the production of acetate ester. In order to determine the precise role of the ATF2 gene in acetate ester production, an ATF2 gene encoding a type of AATase was overexpressed and the ability of the mutant to form acetate esters (including ethyl acetate, isoamyl acetate, and isobutyl acetate) was investigated. The results showed that after 5 days of fermentation, the concentrations of ethyl acetate, isoamyl acetate, and isobutyl acetate in yellow rice wines fermented with EY2 (pUC-PIA2K) increased to 137.79 mg/L (an approximate 4.9-fold increase relative to the parent cell RY1), 26.68 mg/L, and 7.60 mg/L, respectively. This study confirms that the ATF2 gene plays an important role in the production of acetate ester production during Chinese yellow rice wine fermentation, thereby offering prospects for the development of yellow rice wine yeast starter strains with optimized ester-producing capabilities.

  4. [Polycyclic azines with heteroatoms in the 1- and 3-position. 40. Synthesis of heterocyclic immunomodulators. 3. Synthesis of n-1 substituted 3-(2-mercaptoethyl)quinazoline-2,4-(1H,3H)-diones from bis(2-(2-aminobenzoylamino)ethyl)disulfane and testing of immunostimulant activity].

    PubMed

    Gütschow, M; Drössler, K; Leistner, S

    1995-03-01

    A 3-step synthesis, starting from substituted isatoic anhydride was used to prepare substituted 3-(2-mercaptoethyl)quinazoline-2,4(1H,3H)-diones 4. Reaction of 1 with cystamine afforded bis[2-(2-amino-benzoyl-amino)ethyl]disulfanes 2. Reaction of 2 with ethyl chloroformate and subsequent reduction of the heterocyclic disulfanes 3 gave mercaptoethylquinazoline-2,4-diones 4a-f.N-1 methyl and benzyl substituted derivatives 4b and 4c, respectively, show immuno-stimulating activity in various tests.

  5. Antioxidant activity of extracts from Euryale ferox seed.

    PubMed

    Lee, Si Eun; Ju, Eun Mi; Kim, Jeong Hee

    2002-05-31

    Euryale ferox has been widely used in traditional oriental medicine to treat a variety of illness. However, very little is known about the cellular actions by which this plant mediates its therapeutic effects. Various aspects of antioxidant activity were evaluated in total extracts and fractions derived from Euryale ferox. Total extracts (IC50 5.6 microg/ml) showed relatively high level radical scavenging activity toward 1, 1-diphenyl-2-picrylhydrazyl (DPPH) and also enhanced viability of Chinese hamster lung fibroblast (V79-4) cells under exposure to oxidative agents. Upon further fractionation, the highest levels of DPPH radical scavenging and lipid peroxidation inhibitory activities were found in the ethyl acetate and butanol fractions. The ethyl acetate fractions, the butanol fractions, and total extracts of Euryale ferox also dose-dependently enhanced the activities of superoxide dismutase, catalase and glutathione peroxidase in V79-4 cells. Of these three antioxidant enzymes, glutathione peroxidase activity was most strongly induced. Taken together, our findings show that Euryale ferox contains a significant antioxidant activity and that specific components in the ethyl acetate and butanol fractions may play an important role in mediating these antioxidant properties.

  6. Antileishmanial Activity of Handroanthus serratifolius (Vahl) S. Grose (Bignoniaceae)

    PubMed Central

    Costa, Erica Vanessa Souza; Brígido, Heliton Patrick Cordovil; Silva, João Victor da Silva e; Coelho-Ferreira, Marlia Regina; Brandão, Geraldo Célio

    2017-01-01

    This study aimed to evaluate the leishmanicidal activity of ethanol extract, fractions, and isolated substance from Handroanthus serratifolius against Leishmania amazonensis. Furthermore, this activity was related to cytotoxicity, and the selectivity index was determined. The ethanol extract was obtained by maceration of the stem powder, and the extract was subjected to fractionation on chromatographic column. The lapachol was obtained by acid base extraction followed by purification in chromatographic column. The antipromastigote activity and cytotoxicity tests were carried out by the cell viability method (MTT). Modified THP-1 cells were infected with L. amazonensis promastigotes and treated for 24 h with different concentrations of the extract, fractions, and lapachol. The ethanol extract, dichloromethane, and ethyl acetate fractions were not active against promastigotes (IC50 > 200 μg/mL) or cytotoxic (CC50 > 500 μg/mL), and the selectivity index (SI) was greater than 2.5. The ethyl acetate fraction was active only in promastigotes; it is not cytotoxic (CC50 > 500 μg/mL, SI > 5). The lapachol was selectively active only against amastigote (IS > 2.5, CC50 > 500 μg/mL). In summary, lapachol and ethyl acetate fraction are promising against amastigote and promastigote forms, respectively. PMID:28286535

  7. Expression of Acetate Permease-like (apl) Genes in Subsurface Communities of Geobacter Species Under Fluctuating Acetate Concentrations

    SciTech Connect

    Elifantz, H; N'Guessan, A L; Mouser, Paula; Williams, Kenneth H; Wilkins, Michael J; Risso, Carla; Holmes, Dawn; Long, Philip E; Lovley, Derek R

    2010-09-01

    The addition of acetate to uranium-contaminated aquifers in order to stimulate the growth and activity of Geobacter species that reduce uranium is a promising in situ bioremediation option. Optimizing this bioremediation strategy requires that sufficient acetate be added to promote Geobacter species growth. We hypothesized that under acetate-limiting conditions, subsurface Geobacter species would increase the expression of either putative acetate symporters genes (aplI and aplII). Acetate was added to a uranium-contaminated aquifer (Rifle, CO) in two continuous amendments separated by 5 days of groundwater flush to create changing acetate concentrations. While the expression of aplI in monitoring well D04 (high acetate) weakly correlated with the acetate concentration over time, the transcript levels for this gene were relatively constant in well D08 (low acetate). At the lowest acetate concentrations during the groundwater flush, the transcript levels of aplII were the highest. The expression of aplII decreased 2–10-fold upon acetate reintroduction. However, the overall instability of acetate concentrations throughout the experiment could not support a robust conclusion regarding the role of apl genes in response to acetate limitation under field conditions, in contrast to previous chemostat studies, suggesting that the function of a microbial community cannot be inferred based on lab experiments alone.

  8. Expression of acetate permease-like (apl) genes in subsurface communities of Geobacter species under fluctuating acetate concentrations

    SciTech Connect

    Elifantz, H.; N'Guessan, L.A.; Mouser, P.J.; Williams, K H.; Wilkins, M J.; Risso, C.; Holmes, D.E.; Long, P.E.; Lovley, D.R.

    2010-03-01

    The addition of acetate to uranium-contaminated aquifers in order to stimulate the growth and activity of Geobacter species that reduce uranium is a promising in situ bioremediation option. Optimizing this bioremediation strategy requires that sufficient acetate be added to promote Geobacter species growth. We hypothesized that under acetate-limiting conditions, subsurface Geobacter species would increase the expression of either putative acetate symporters genes (aplI and aplII). Acetate was added to a uranium-contaminated aquifer (Rifle, CO) in two continuous amendments separated by 5 days of groundwater flush to create changing acetate concentrations. While the expression of aplI in monitoring well D04 (high acetate) weakly correlated with the acetate concentration over time, the transcript levels for this gene were relatively constant in well D08 (low acetate). At the lowest acetate concentrations during the groundwater flush, the transcript levels of aplII were the highest. The expression of aplII decreased 2-10-fold upon acetate reintroduction. However, the overall instability of acetate concentrations throughout the experiment could not support a robust conclusion regarding the role of apl genes in response to acetate limitation under field conditions, in contrast to previous chemostat studies, suggesting that the function of a microbial community cannot be inferred based on lab experiments alone.

  9. Ethnobotany, chemical constituents and biological activities of the flowers of Hydnora abyssinica A.Br. (Hydnoraceae).

    PubMed

    Al-Fatimi, M; Ali, N A A; Kilian, N; Franke, K; Arnold, N; Kuhnt, C; Schmidt, J; Lindequist, U

    2016-04-01

    Hydnora abyssinica A.Br. (Hydnoraceae), a holoparasitic herb, is for the first time recorded for Abyan governorate of South Yemen. Flowers of this species were studied for their ethnobotanical, biological and chemical properties for the first time. In South Yemen, they are traditionally used as wild food and to cure stomach diseases, gastric ulcer and cancer. Phytochemical analysis of the extracts showed the presence of terpenes, tannins, phenols, and flavonoids. The volatile components of the air-dried powdered flowers were identified using a static headspace GC/MS analysis as acetic acid, ethyl acetate, sabinene, α-terpinene, (+)-D-limonene and γ-terpinene. These volatile compounds that characterize the odor and taste of the flowers were detected for the first time in a species of the family Hydnoraceae. The flowers were extracted by n-hexane, dichlormethane, ethyl acetate, ethanol, methanol and water. With exception of the water extract all extracts demonstrated activities against Gram-positive bacteria as well as remarkable radical scavenging activities in DPPH assay. Ethyl acetate, methanol and water extracts exhibited good antifungal activities. The cytotoxic activity of the extracts against FL cells, measured in neutral red assay, was only weak (IC50 > 500 μg/mL). The results justify the traditional use of the flowers of Hydnora abyssinica in South Yemen.

  10. Molluscicidal activity of Aglaia duperreana and the constituents of its twigs and leaves.

    PubMed

    Zhang, Heng; Xu, Han-Hong; Song, Zhi-Jun; Chen, Lin-Yan; Wen, Hao-Ju

    2012-09-01

    The methanol (MeOH) extract of the twigs and leaves of Aglaia duperreana was investigated for its molluscicidal activity against Pomacea canaliculata. The extract was found to exhibit significant molluscicidal activity. The ethyl acetate soluble fraction of the extract showed the most potent molluscicidal activity among different solvent fractions. The bioactivity-guided chemical investigation of the ethyl acetate soluble fraction led to a new triterpenoid along with 15 known compounds. Their structures were elucidated by spectroscopic methods, including one- and two-dimensional nuclear magnetic resonance techniques as well as mass spectroscopic analysis. The molluscicidal activities of compounds 2-16 against P. canaliculata were also investigated. Naringenin trimethyl ether showed significant molluscicidal activity with a median lethal concentration (LC(50)) of 3.9 μg/mL, which was indicated higher potency than the positive control, tea saponin (LC(50)=4.5 μg/mL).

  11. Manuka Honey Exerts Antioxidant and Anti-Inflammatory Activities That Promote Healing of Acetic Acid-Induced Gastric Ulcer in Rats

    PubMed Central

    Almasaudi, Saad B.; Al-Hindi, Rashad R.; Abdel-dayem, Umama A.; Ali, Soad S.; Saleh, Rasha M.; Al Jaouni, Soad K.

    2017-01-01

    Gastric ulcers are a major problem worldwide with no effective treatment. The objective of this study was to evaluate the use of manuka honey in the treatment of acetic acid-induced chronic gastric ulcers in rats. Different groups of rats were treated with three different concentrations of honey. Stomachs were checked macroscopically for ulcerative lesions in the glandular mucosa and microscopically for histopathological alterations. Treatment with manuka honey significantly reduced the ulcer index and maintained the glycoprotein content. It also reduced the mucosal myeloperoxidase activity, lipid peroxidation (MDA), and the inflammatory cytokines (TNF-α, IL-1β, and IL-6) as compared to untreated control group. In addition, honey-treated groups showed significant increase in enzymatic (GPx and SOD) and nonenzymatic (GSH) antioxidants besides levels of the anti-inflammatory cytokine IL-10. Flow cytometry studies showed that treatment of animals with manuka honey has normalized cell cycle distribution and significantly lowered apoptosis in gastric mucosa. In conclusion, the results indicated that manuka honey is effective in the treatment of chronic ulcer and preservation of mucosal glycoproteins. Its effects are due to its antioxidant and anti-inflammatory properties that resulted in a significant reduction of the gastric mucosal MDA, TNF-α, IL-1β, and IL-6 and caused an elevation in IL-10 levels. PMID:28250794

  12. Simultaneous structure-activity studies and arming of natural products by C–H amination reveal cellular targets of eupalmerin acetate

    PubMed Central

    Li, Jing; Cisar, Justin S.; Zhou, Congying; Vera, Brunilda; Williams, Howard; Rodríguez, Abimael D.; Cravatt, Benjamin F.; Romo, Daniel

    2014-01-01

    To fully exploit the inherent and enduring potential of natural products for fundamental cell biology and drug lead discovery, synthetic methods for functionalizing unique sites are highly desirable. Here we describe a strategy for the derivatization of natural products at ‘unfunctionalized’ positions via Rh(II)-catalyzed amination enabling simultaneous structure-activity relationship (SAR) studies and arming (alkynylation) of natural products. Employing Du Bois C–H amination, allylic and benzylic C–H bonds underwent amination and olefins underwent aziridination. With tertiary amine-containing natural products, amidines were produced via C–H amination/oxidation and unusual N-aminations provided hydrazine sulfamate inner salts. The alkynylated derivatives are readied for subsequent conjugation to access cellular probes for mechanism of action studies. Both chemo- and site-selectivity was studied by application to a diverse set of natural products including the marine-derived anticancer diterpene, eupalmerin acetate (EPA). Quantitative proteome profiling with an alkynyl EPA derivative obtained by site-selective, allylic C–H amination led to identification of several protein targets in HL-60 cells, including several known to be associated with cancer proliferation, suggestive of a polypharmacological mode of action for EPA. PMID:23695633

  13. Altered architecture and enhanced drought tolerance in rice via the down-regulation of indole-3-acetic acid by TLD1/OsGH3.13 activation.

    PubMed

    Zhang, Sheng-Wei; Li, Chen-Hui; Cao, Jia; Zhang, Yong-Cun; Zhang, Su-Qiao; Xia, Yu-Feng; Sun, Da-Ye; Sun, Ying

    2009-12-01

    Plant architecture is determined by genetic and developmental programs as well as by environmental factors. Sessile plants have evolved a subtle adaptive mechanism that allows them to alter their growth and development during periods of stress. Phytohormones play a central role in this process; however, the molecules responsible for integrating growth- and stress-related signals are unknown. Here, we report a gain-of-function rice (Oryza sativa) mutant, tld1-D, characterized by (and named for) an increased number of tillers, enlarged leaf angles, and dwarfism. TLD1 is a rice GH3.13 gene that encodes indole-3-acetic acid (IAA)-amido synthetase, which is suppressed in aboveground tissues under normal conditions but which is dramatically induced by drought stress. The activation of TLD1 reduced the IAA maxima at the lamina joint, shoot base, and nodes, resulting in subsequent alterations in plant architecture and tissue patterning but enhancing drought tolerance. Accordingly, the decreased level of free IAA in tld1-D due to the conjugation of IAA with amino acids greatly facilitated the accumulation of late-embryogenesis abundant mRNA compared with the wild type. The direct regulation of such drought-inducible genes by changes in the concentration of IAA provides a model for changes in plant architecture via the process of drought adaptation, which occurs frequently in nature.

  14. Preparation of a novel PAN/cellulose acetate-Ag based activated carbon nanofiber and its adsorption performance for low-concentration SO2

    NASA Astrophysics Data System (ADS)

    Wu, Yan-bo; Bi, Jun; Lou, Ting; Song, Tie-ben; Yu, Hong-quan

    2015-04-01

    Polyacrylonitrile (PAN), PAN/cellulose acetate (CA), and PAN/CA-Ag based activated carbon nanofiber (ACNF) were prepared using electrostatic spinning and further heat treatment. Thermogravimetry-differential scanning calorimetry (TG-DSC) analysis indicated that the addition of CA or Ag did not have a significant impact on the thermal decomposition of PAN materials but the yields of fibers could be improved. Scanning electron microscopy (SEM) analysis showed that the micromorphologies of produced fibers were greatly influenced by the viscosity and conductivity of precursor solutions. Fourier transform infrared spectroscopy (FT-IR) analysis proved that a cyclized or trapezoidal structure could form and the carbon scaffold composed of C=C bonds appeared in the PAN-based ACNFs. The characteristic diffraction peaks in X-ray diffraction (XRD) spectra were the evidence of a turbostratic structure and silver existed in the PAN/CA-Ag based ACNF. Brunner-Emmett-Teller (BET) analysis showed that the doping of CA and Ag increased surface area and micropore volume of fibers; particularly, PAN/CA-Ag based ACNF exhibited the best porosity feature. Furthermore, SO2 adsorption experiments indicated that all the three fibers had good adsorption effects on lower concentrations of SO2 at room temperature; especially, the PAN/CA-Ag based ACNF showed the best adsorption performance, and it may be one of the most promising adsorbents used in the fields of chemical industry and environment protection.

  15. [Experimental study of proflavine acetate phototransformation processes].

    PubMed

    Zholdakova, Z I; Sinitsyna, O O; Lebedev, A T; Kharchevnikova, N V

    2009-01-01

    Changes in proflavine acetate phototransformation processes upon exposure to visible-range irradiation were studied by high performance liquid chromatography. Proflavine acetate was offered as a photosensitizer during photodynamic water disinfection. Dye transformation products upon time-varying exposure to irradiation were identified. By using structure-activity relationships and information from toxicity databases, the authors evaluated the hazard of the identified products and identified the most hazardous ones.

  16. Intrarenal dopamine attenuates deoxycorticosterone acetate/high salt-induced blood pressure elevation in part through activation of a medullary cyclooxygenase 2 pathway.

    PubMed

    Yao, Bing; Harris, Raymond C; Zhang, Ming-Zhi

    2009-11-01

    Locally produced dopamine in the renal proximal tubule inhibits salt and fluid reabsorption, and a dysfunctional intrarenal dopaminergic system has been reported in essential hypertension and experimental hypertension models. Using catechol-O-methyl-transferase knockout (COMT(-/-)) mice, which have increased renal dopamine because of deletion of the major renal dopamine-metabolizing enzyme, we investigated the effect of intrarenal dopamine on the development of hypertension in the deoxycorticosterone acetate/high-salt (DOCA/HS) model. DOCA/HS led to significant increases in systolic blood pressure in wild-type mice (from 115+/-2 to 153+/-4 mm Hg), which was significantly attenuated in COMT(-/-) mice (from 114+/-2 to 135+/-3 mm Hg). In DOCA/HS COMT(-/-) mice, the D1-like receptor antagonist SCH-23390 increased systolic blood pressure (156+/-2 mm Hg). DOCA/HS COMT(-/-) mice also exhibited more urinary sodium excretion (COMT(-/-) versus wild-type: 3038+/-430 versus 659+/-102 micromol/L per 24 hours; P<0.01). Furthermore, DOCA/HS-induced renal oxidative stress was significantly attenuated in COMT(-/-) mice. COX-2-derived prostaglandins in the renal medulla promote sodium excretion, and dopamine stimulates medullary prostaglandin production. Renal medullary COX-2 expression and urinary prostaglandin E2 excretion were significantly higher in COMT(-/-) than in wild-type mice after DOCA/HS treatment. In DOCA/HS-treated COMT(-/-) mice, the COX-2 inhibitor SC-58236 reduced urinary sodium and prostaglandin E(2) excretion and increased systolic blood pressure (153+/-2 mm Hg). These studies indicate that an activated renal dopaminergic system attenuates the development of hypertension, at least in large part through activating medullary COX-2 expression/activity, and also decreases oxidative stress resulting from DOCA/HS.

  17. Acyclonucleosides, modified seco-nucleosides, and salicyl- or catechol-derived acyclic 5-fluorouracil O,N-acetals: antiproliferative activities, cellular differentiation and apoptosis.

    PubMed

    Marchal, Juan A; Núñez, María C; Aránega, Antonia; Gallo, Miguel A; Espinosa, Antonio; Campos, Joaquín M

    2009-01-01

    The goal of cancer chemotherapy with classical drugs - the destruction of the tumor cells - is often complicated by significant toxicity. As an alternative, induced differentiation modulates the cell programme by transforming malignant cells into mature cells with no proliferative potential. Our data demonstrate that (+/-)-1-{[3-(2-hydroxyethoxy)-1-isopropoxy]propyl}-5-fluorouracil inhibits proliferation, induces myogenic differentiation, increases the expression of proteins specifically present in normally differentiated skeletal muscle cells, and modifies the adhesion capacity of these cells against the rhabdomyosarcoma cell line RD. From a designing point of view, a benzene ring was fused to the side chain in order to increase the lipophilicity and anticancer activity of our molecules. Herein we report the preparation and biological activity of three compounds having the general formula (+/-)-1-[2-(5-substituted-2-hydroxybenzyloxy)-1-methoxyethyl]-5-fluorouracils. A catechol-derived compound such as (+/-)-1-[3-(2-hydroxyphenoxy)-1-methoxypropyl]-5-fluorouracil and two salicyl-derived compounds such as (+/-)-(Z)-1-[4-(2-hydroxyphenyl)-1-methoxy-but-3-enyl]-5-fluorouracil [(Z)-43] and its dihydrogenated derivative (+/-)-1-[4-(2-hydroxyphenyl)-1-methoxybutyl]-5-fluorouracil were prepared to complete the set of six O,N-acetals. The most active compound against the MCF-7 breast cancer cell line was (+/-)-(Z)-43 with an IC(50) = 9.40 +/- 0.64 microM. Differentiated breast cancer cells generate fat deposits within the cytoplasm. The MCF-7 cells trea-ed with (+/-)-(Z)-43 caused an increase in the lipid content over control cells after 3 days of treatment. Our results suggest that there may be significant potential advantages in the use of this new differentiating agent for the treatment of breast cancer.

  18. Yeast growth in raffinose results in resistance to acetic-acid induced programmed cell death mostly due to the activation of the mitochondrial retrograde pathway.

    PubMed

    Guaragnella, Nicoletta; Zdralević, Maša; Lattanzio, Paolo; Marzulli, Domenico; Pracheil, Tammy; Liu, Zhengchang; Passarella, Salvatore; Marra, Ersilia; Giannattasio, Sergio

    2013-12-01

    In order to investigate whether and how a modification of mitochondrial metabolism can affect yeast sensitivity to programmed cell death (PCD) induced by acetic acid (AA-PCD), yeast cells were grown on raffinose, as a sole carbon source, which, differently from glucose, favours mitochondrial respiration. We found that, differently from glucose-grown cells, raffinose-grown cells were mostly resistant to AA-PCD and that this was due to the activation of mitochondrial retrograde (RTG) response, which increased with time, as revealed by the up-regulation of the peroxisomal isoform of citrate synthase and isocitrate dehydrogenase isoform 1, RTG pathway target genes. Accordingly, the deletion of RTG2 and RTG3, a positive regulator and a transcription factor of the RTG pathway, resulted in AA-PCD, as shown by TUNEL assay. Neither deletion in raffinose-grown cells of HAP4, encoding the positive regulatory subunit of the Hap2,3,4,5 complex nor constitutive activation of the RTG pathway in glucose-grown cells due to deletion of MKS1, a negative regulator of RTG pathway, had effect on yeast AA-PCD. The RTG pathway was found to be activated in yeast cells containing mitochondria, in which membrane potential was measured, capable to consume oxygen in a manner stimulated by the uncoupler CCCP and inhibited by the respiratory chain inhibitor antimycin A. AA-PCD resistance in raffinose-grown cells occurs with a decrease in both ROS production and cytochrome c release as compared to glucose-grown cells en route to AA-PCD.

  19. Phosphine-catalyzed reactions of activated olefins tethered to cycloalkanones. substrate- and solvent-controlled synthesis of bicyclo[3.2.1]octanones, mixed acetals, and Morita-Baylis-Hillman products.

    PubMed

    Wang, Yanhui; Jaunet, Alexis; Geoffroy, Philippe; Miesch, Michel

    2013-12-20

    The n-Bu3P organocatalyzed reaction of cycloalkanones, i.e., cyclopentanones or 1,3-cyclopentanediones tethered to actived olefins, afforded selectively and in high yields three different types of products: bicyclo[3.2.1]octanones, mixed acetals, and Morita-Baylis-Hillman products. The progress of the reaction was closely related to the reaction medium and to the length of the tether located between the cyclopentanone (-dione) and the activated olefin.

  20. Design and Evaluation of Ethyl Cellulose Based Matrix Tablets of Ibuprofen with pH Modulated Release Kinetics

    PubMed Central

    Chandran, S.; Asghar, Laila F. A.; Mantha, Neelima

    2008-01-01

    Controlled release preparations have been reported to reduce the gastro irritant and ulcerogenic effects of non steroidal antiinflammatory drugs. In the present study, an attempt was made to develop matrix tablet-based controlled release formulations of ibuprofen, using ethyl cellulose as the rate-controlling polymer. In order to prevent initial release of the drug in the acidic environment of the stomach, cellulose acetate phthalate was incorporated in the matrix in varying amounts. It was found that with increasing the proportion of ethyl cellulose in the matrix, the drug release was extended for 14-16 h. Incorporation of cellulose acetate phthalate in ethyl cellulose matrix provided very low initial release of the drug in the first 2-3 h followed by enhanced release rate in alkaline medium owing to the high solubility of cellulose acetate phthalate at basic pH which led to creation of a porous matrix. It was concluded that combination of cellulose acetate phthalate with ethyl cellulose in the matrix base can be an effective means of developing a controlled release formulation of ibuprofen with very low initial release followed with controlled release up to 14-16 h. PMID:21394255

  1. Anti-inflammatory activity of Heliotropium strigosum in animal models.

    PubMed

    Khan, Haroon; Khan, Murad Ali; Gul, Farah; Hussain, Sajjid; Ashraf, Nadeem

    2015-12-01

    The current project was designed to evaluate the anti-inflammatory activity of crude extract of Heliotropium strigosum and its subsequent solvent fractions in post carrageenan-induced edema and post xylene-induced ear edema at 50, 100, and 200 mg/kg intraperitoneally. The results revealed marked attenuation of edema induced by carrageenan injection in a dose-dependent manner. The ethyl acetate fraction was most dominant with 73.33% inhibition followed by hexane fraction (70.66%). When the extracts were challenged against xylene-induced ear edema, again ethyl acetate and hexane fractions were most impressive with 38.21 and 35.77% inhibition, respectively. It is concluded that various extracts of H. strigosum possessed strong anti-inflammatory activity in animal models.

  2. Thalidomide increases both intra-tumoural tumour necrosis factor-α production and anti-tumour activity in response to 5,6-dimethylxanthenone-4-acetic acid

    PubMed Central

    Cao, Z; Joseph, W R; Browne, W L; Mountjoy, K G; Palmer, B D; Baguley, B C; Ching, L-M

    1999-01-01

    5,6-Dimethylxanthenone-4-acetic acid (DMXAA), synthesized in this laboratory and currently in phase I clinical trial, is a low molecular weight inducer of tumour necrosis factor-α (TNF-α). Administration of DMXAA to mice with established transplantable tumours elicits rapid vascular collapse selectively in the tumour, followed by extensive haemorrhagic necrosis mediated primarily through the production of TNF-α. In this report we have investigated the synthesis of TNF-α mRNA in hepatic, splenic and tumour tissue. Co-administration of thalidomide with DMXAA increased anti-tumour activity and increased intra-tumoural TNF-α production approximately tenfold over that obtained with DMXAA alone. Thalidomide increased splenic TNF-α production slightly but significantly decreased serum and hepatic levels of TNF-α induced with DMXAA. Lipopolysaccharide (LPS) induced 300-fold higher serum TNF-α than did DMXAA at the maximum tolerated dose, but induced similar amounts of TNF-α in spleen, liver and tumour. Splenic TNF-α activity induced with LPS was slightly increased with thalidomide, but serum and liver TNF-α levels were suppressed. Thalidomide did not increase intra-tumoural TNF-α production induced with LPS, in sharp contrast to that obtained with DMXAA. While thalidomide improved the anti-tumour response to DMXAA, it had no effect on the anti-tumour action of LPS that did not induce a significant growth delay or cures against the Colon 38 tumour. The increase in the anti-tumour action by thalidomide in combination with DMXAA corresponded to an increase in intra-tumoural TNF-α production. Co-administration of thalidomide may represent a novel approach to improving selective intra-tumoural TNF-α production and anti-tumour efficacy of DMXAA. © 1999 Cancer Research Campaign PMID:10360649

  3. Synthesis, characterization and evaluation of antibacterial activity of (E)-N'-(substituted benzylidene)-2-(2-fluorobenzyl)-5-ethyl-2H-1,2,3-triazole-4-carbohydrazides.

    PubMed

    Reddy, P V B; Kamala Prasad, V; Manjunath, G; Venkata Ramana, P

    2016-09-01

    Triazoles and their derivatives are important precursors in the pharmacological field due to their broad diversity of medicinal and biological deed. In this article, the exploration is to put an effort to produce some novel biologically active triazole 4-carbohydrazide derivatives. The structures of the newly synthesized compounds were characterized and confirmed by spectral data and were screened for anti-bacterial activity. Compounds 5(d-i), 5l and 5m were observed to possess potent anti-microbial activity.

  4. Bacillus coagulans tolerance to 1-ethyl-3-methylimidazolium-based ionic liquids in aqueous and solid-state thermophilic culture.

    PubMed

    Simmons, Christopher W; Reddy, Amitha P; Vandergheynst, Jean S; Simmons, Blake A; Singer, Steven W

    2014-01-01

    The use of ionic liquids (ILs) to disrupt the recalcitrant structure of lignocellulose and make polysaccharides accessible to hydrolytic enzymes is an emerging technology for biomass pretreatment in lignocellulosic biofuel production. Despite efforts to reclaim and recycle IL from pretreated biomass, residual IL can be inhibitory to microorganisms used for downstream fermentation. As a result, pathways for IL tolerance are needed to improve the activity of fermentative organisms in the presence of IL. In this study, microbial communities from compost were cultured under high-solids and thermophilic conditions in the presence of 1-ethyl-3-methylimidazolium-based ILs to enrich for IL-tolerant microorganisms. A strain of Bacillus coagulans isolated from an IL-tolerant community was grown in liquid and solid-state culture in the presence of the ILs 1-ethyl-3-methylimidazolium acetate ([C2mim][OAc]) or 1-ethyl-3-methylimidazolium chloride ([C2mim][Cl]) to gauge IL tolerance. Viability and respiration varied with the concentration of IL applied and the type of IL used. B. coagulans maintained growth and respiration in the presence of 4 wt% IL, a concentration similar to that present on IL-pretreated biomass. In the presence of both [C2mim][OAc] and [C2mim][Cl] in liquid culture, B. coagulans grew at a rate approximately half that observed in the absence of IL. However, in solid-state culture, the bacteria were significantly more tolerant to [C2mim][Cl] compared with [C2mim][OAc]. B. coagulans tolerance to IL under industrially relevant conditions makes it a promising bacterium for understanding mechanisms of IL tolerance and discovering IL tolerance pathways for use in other microorganisms, particularly those used in bioconversion of IL-pretreated plant biomass.

  5. Oxidation of indole-3-acetic acid to oxindole-3-acetic acid by an enzyme preparation from Zea mays

    NASA Technical Reports Server (NTRS)

    Reinecke, D. M.; Bandurski, R. S.

    1988-01-01

    Indole-3-acetic acid is oxidized to oxindole-3-acetic acid by Zea mays tissue extracts. Shoot, root, and endosperm tissues have enzyme activities of 1 to 10 picomoles per hour per milligram protein. The enzyme is heat labile, is soluble, and requires oxygen for activity. Cofactors of mixed function oxygenase, peroxidase, and intermolecular dioxygenase are not stimulatory to enzymic activity. A heat-stable, detergent-extractable component from corn enhances enzyme activity 6- to 10-fold. This is the first demonstration of the in vitro enzymic oxidation of indole-3-acetic acid to oxindole-3-acetic acid in higher plants.

  6. Branchial and renal pathology in the fish exposed chronically to methoxy ethyl mercuric chloride

    SciTech Connect

    Gill, T.S.; Pant, J.C.; Tewari, H.

    1988-08-01

    Pathological manifestations causally related to pesticide poisoning have been described in both surficial and internal tissues of the fishes. Among the various organomercurials are phenyl mercuric acetate, methyl mercuric dicyanidiamide, methoxy ethyl mercuric chloride, methoxy ethyl mercuric silicate etc. Of these, the methoxy ethyl mercuric chloride (MEMC) is used in agriculture as an antifungal seed dressing, and its toxicity is primarily manifest in the Hg/sup 2 +/ ion. This report describes pathogenesis of branchial and renal lesions in the common freshwater fish, Puntius conchonius exposed chronically to sublethal levels of MEMC. Prior to this, alterations in the peripheral blood and metabolite levels in response to experimental MEMC poisoning have been demonstrated in this species.

  7. Synthesis and Characterization of Novel Cu(II), Pd(II) and Pt(II) Complexes with 8-Ethyl-2-hydroxytricyclo(7.3.1.0(2,7))tridecan-13-one-thiosemicarbazone: Antimicrobial and in Vitro Antiproliferative Activity.

    PubMed

    Pahonțu, Elena; Paraschivescu, Codruța; Ilieș, Diana-Carolina; Poirier, Donald; Oprean, Camelia; Păunescu, Virgil; Gulea, Aurelian; Roșu, Tudor; Bratu, Ovidiu

    2016-05-21

    New Cu(II), Pd(II) and Pt(II) complexes, (Cu(L)(H₂O)₂(OAc)) (1), (Cu(HL)(H₂O)₂(SO₄)) (2), (Cu(L)(H₂O)₂(NO₃)) (3), (Cu(L)(H₂O)₂(ClO₄)) (4), (Cu(L)₂(H₂O)₂) (5), (Pd(L)(OAc))H₂O (6), and (Pt(L)₂) (7) were synthesized from 8-ethyl-2-hydroxytricyclo(7.3.1.0(2,7))tridecan-13-one thiosemicarbazone (HL). The ligand and its metal complexes were characterized by IR, ¹H-NMR, (13)C-NMR, UV-Vis, FAB, EPR, mass spectroscopy, elemental and thermal analysis, magnetic susceptibility measurements and molar electric conductivity. The free ligand and the metal complexes have been tested for their antimicrobial activity against E. coli, S. enteritidis, S. aureus, E. faecalis, C. albicans and cytotoxicity against the NCI-H1573 lung adenocarcinoma, SKBR-3 human breast, MCF-7 human breast, A375 human melanoma and HL-60 human promyelocytic leukemia cell lines. Copper complex 2 exhibited the best antiproliferative activities against MCF-7 human breast cancer cells. A significant inhibition of malignant HL-60 cell growth was observed for copper complex 2, palladium complex 6 and platinum complex 7, with IC50 values of 1.6 µM, 6.5 µM and 6.4 µM, respectively.

  8. Tor-Sch9 deficiency activates catabolism of the ketone body-like acetic acid to promote trehalose accumulation and longevity.

    PubMed

    Hu, Jia; Wei, Min; Mirzaei, Hamed; Madia, Federica; Mirisola, Mario; Amparo, Camille; Chagoury, Shawna; Kennedy, Brian; Longo, Valter D

    2014-06-01

    In mammals, extended periods of fasting leads to the accumulation of blood ketone bodies including acetoacetate. Here we show that similar to the conversion of leucine to acetoacetate in fasting mammals, starvation conditions induced ketone body-like acetic acid generation from leucine in S. cerevisiae. Whereas wild-type and ras2Δ cells accumulated acetic acid, long-lived tor1Δ and sch9Δ mutants rapidly depleted it through a mitochondrial acetate CoA transferase-dependent mechanism, which was essential for lifespan extension. The sch9Δ-dependent utilization of acetic acid also required coenzyme Q biosynthetic genes and promoted the accumulation of intracellular trehalose. These results indicate that Tor-Sch9 deficiency extends longevity by switching cells to an alternative metabolic mode, in which acetic acid can be utilized for the storage of stress resistance carbon sources. These effects are reminiscent of those described for ketone bodies in fasting mammals and raise the possibility that the lifespan extension caused by Tor-S6K inhibition may also involve analogous metabolic changes in higher eukaryotes.

  9. Acetic acid production from food wastes using yeast and acetic acid bacteria micro-aerobic fermentation.

    PubMed

    Li, Yang; He, Dongwei; Niu, Dongjie; Zhao, Youcai

    2015-05-01

    In this study, yeast and acetic acid bacteria strains were adopted to enhance the ethanol-type fermentation resulting to a volatile fatty acids yield of 30.22 g/L, and improve acetic acid production to 25.88 g/L, with food wastes as substrate. In contrast, only 12.81 g/L acetic acid can be obtained in the absence of strains. The parameters such as pH, oxidation reduction potential and volatile fatty acids were tested and the microbial diversity of different strains and activity of hydrolytic ferment were investigated to reveal the mechanism. The optimum pH and oxidation reduction potential for the acetic acid production were determined to be at 3.0-3.5 and -500 mV, respectively. Yeast can convert organic matters into ethanol, which is used by acetic acid bacteria to convert the organic wastes into acetic acid. The acetic acid thus obtained from food wastes micro-aerobic fermentation liquid could be extracted by distillation to get high-pure acetic acid.

  10. In vitro Evaluation of Anthelmintic Activity of Nauclea orientalis Leaves

    PubMed Central

    Raghavamma, S. T. V.; Rao, N. Rama

    2010-01-01

    Antianthelmintic activity of successive extracts (chloroform, acetone, ethanol and aqueous) of Nauclea orientalis leaves were evaluated separately on adult Indian earthworm (Pheretima posthuma) and compared with that of albendazole. It was found that the extracts exhibited, respectively dose-dependent action and inhibition of spontaneous motility (paralysis) and death of earthworms. The results indicated that the chloroform, ethyl acetate and ethanol extracts were more potent. PMID:21218070

  11. Acquired resistance to rechallenge injury in rats recovered from subclinical renal damage with uranyl acetate-Importance of proliferative activity of tubular cells

    SciTech Connect

    Sun, Yuan; Fujigaki, Yoshihide; Sakakima, Masanori; Hishida, Akira

    2010-02-15

    Animals recovered from acute renal failure are resistant to subsequent insult. We investigated whether rats recovered from mild proximal tubule (PT) injury without renal dysfunction (subclinical renal damage) acquire the same resistance. Rats 14 days after recovering from subclinical renal damage, which was induced by 0.2 mg/kg of uranyl acetate (UA) (sub-toxic dose), were rechallenged with 4 mg/kg of UA (nephrotoxic dose). Fate of PT cells and renal function were examined in response to nephrotoxic dose of UA. All divided cells after sub-toxic dose of UA insult were labeled with bromodeoxyuridine (BrdU) for 14 days then the number of PT cells with or without BrdU-labeling was counted following nephrotoxic dose of UA insult. Rats recovered from subclinical renal damage gained resistance to nephrotoxic dose of UA with reduced renal dysfunction, less severity of peak damage (necrotic and TUNEL+ apoptotic cells) and accelerated PT cell proliferation, but with earlier peak of PT damage. The decrease in number of PT cells in the early phase of rechallenge injury with nephrotoxic UA was more in rats pretreated with sub-toxic dose of UA than vehicle pretreated rats. The exaggerated loss of PT cells was mainly caused by the exaggerated loss of BrdU+ divided cells. In contrast, accelerated cell proliferation in rats recovered from sub-toxic dose of UA was observed mainly in BrdU- non-divided cells. The findings suggest that rats recovered from subclinical renal damage showed partial acquired resistance to nephrotoxic insult. Accelerated recovery with increased proliferative activity of non-divided PT cells after subclinical renal damage may mainly contribute to acquired resistance.

  12. Costus afer Possesses Carbohydrate Hydrolyzing Enzymes Inhibitory Activity and Antioxidant Capacity In Vitro

    PubMed Central

    Tchamgoue, Armelle D.; Tchokouaha, Lauve R. Y.; Tarkang, Protus A.; Kuiate, Jules-Roger; Agbor, Gabriel A.

    2015-01-01

    Diabetes mellitus is a metabolic disorder of glucose metabolism which correlates with postprandial hyperglycemia and oxidative stress. Control of blood glucose level is imperative in the management of diabetes. The present study tested the hypothesis that Costus afer, an antihyperglycemic medicinal plant, possesses inhibitory activity against carbohydrate hydrolyzing enzymes. Hexane, ethyl acetate, methanol, and water extracts were prepared from the leaf, stem, and rhizome of C. afer and subjected to phytochemical screening, assayed for α-amylase and α-glucosidase inhibitory activities and antioxidant capacity (determined by total phenolic and total flavonoids contents, ferric reducing antioxidant power (FRAP), and DPPH radical scavenging activity). All extracts inhibited α-amylase and α-glucosidase activities. Ethyl acetate rhizome and methanol leaf extracts exhibited the best inhibitory activity against α-amylase and α-glucosidase (IC50: 0.10 and 5.99 mg/mL), respectively. Kinetic analysis revealed two modes of enzyme inhibition (competitive and mixed). All extracts showed antioxidant capacity, with hexane extracts exhibiting the best activity. DPPH assay revealed that methanol leaf, rhizome, and ethyl acetate stem extracts (IC50 < 5 mg/mL) were the best antioxidants. The presence of bioactive compounds such as flavonoids, alkaloids, phenols, and tannins may account for the antioxidant capacity and carbohydrate hydrolyzing enzyme inhibitory activity of C. afer. PMID:26246844

  13. Evaluation of in-vitro antibacterial activity and anti-inflammatory activity for different extracts of Rauvolfia tetraphylla L. root bark

    PubMed Central

    Ganga Rao, B.; Umamaheswara Rao, P.; Sambasiva Rao, E.; Mallikarjuna Rao, T.; Praneeth. D, V. S.

    2012-01-01

    Objective To assess the in-vitro antibacterial activity and anti-inflammatory activity of orally administered different extracts (Hydro-alcoholic, methanolic, ethyl acetate and hexane) of Rauvolfia tetraphylla (R. tetraphylla) root bark in Carrageenan induced acute inflammation in rats. Methods In-vitro antibacterial activity was evaluated for extracts against four Gram positive and four Gram negative bacteria by using cylinder plate assay. Hydro-alcoholic extract (70% v/v ethanol) at 200, 400 and 800 mg/kg doses and methanolic, ethyl acetate and hexane extracts at doses 100, 200 and 400 mg/kg were tested for anti-inflammatory activity in Carrageenan induced rat paw oedema model and paw thickness was measured every one hour up to 6 hrs. Results All extracts of R. tetraphylla root bark showed good zone of inhibition against tested bacterial strains. In Carrageenan induced inflammation model, hydro-alcoholic and methanolic extract of R. tetraphylla root bark at three different doses produced significant (P<0.001) reduction when compared to vehicle treated control group and hexane, ethyl acetate extracts. Conclusions In the present study extracts of R. tetraphylla root bark shows good in-vitro antibacterial activity and in-vivo anti-inflammatory activity in rats. PMID:23569853

  14. In vitro antioxidant, lipoxygenase and xanthine oxidase inhibitory activities of fractions from Cienfuegosia digitata Cav., Sida alba L. and Sida acuta Burn f. (Malvaceae).

    PubMed

    Konaté, K; Souza, A; Coulibaly, A Y; Meda, N T R; Kiendrebeogo, M; Lamien-Meda, A; Millogo-Rasolodimby, J; Lamidi, M; Nacoulma, O G

    2010-11-15

    In this study polyphenol content, antioxidant activity, lipoxygenase (LOX) and Xanthine Oxidase (XO) inhibitory effects of n-hexane, dichloromethane, ethyl acetate and n-butanol fractions of aqueous acetone extracts from S. alba L., S. acuta Burn f and Cienfuegosia digitata Cav. were investigated. The total phenolics, flavonoids, flavonols and total tannins were determined by spectrophotometric methods using Folin-ciocalteu, AlCl3 reagents and tannic acid, respectively. The antioxidant potential was evaluated using three methods: inhibition of free radical 2,2-diphenyl-1-picrylhydramzyl (DPPH), ABTS radical cation decolorization assay and Iron (III) to iron (II) reduction activity (FRAP). For enzymatic activity, lipoxygenase and xanthine oxidase inhibitory activities were used. This study shows a relationship between polyphenol contents, antioxidant and enzymatic activities. Present results showed that ethyl acetate and dichloromethane fractions elicit the highest polyphenol content, antioxidant and enzymatic activities.

  15. Test for Chemical Induction of Chromosome Aberrations in Cultured Chinese Hamster Ovary (CHO) Cells With and Without Metabolic Activation. Test Article: Dimethylamine-2-2ethyl azide (DMAZ)

    DTIC Science & Technology

    2008-07-26

    01’ per mg CPA Dilutions of the sample S9, ranging from 0.2 - 10% in S9 mix, were tested for their ability to activate benzo ( a ) pyrene (BP) and 2...be subject to a penalty for failing to comply with a collection of information if it does not display a currently valid OMB control number. 1...concentrations of 10, 50, 100, 500, 1000, 2500, and 5000 ?g/mL in both with and without activation and was found negative for clastogenic potential. A

  16. Mode of action of ethyl tertiary-butyl ether hepatotumorigenicity in the rat: evidence for a role of oxidative stress via activation of CAR, PXR and PPAR signaling pathways.

    PubMed

    Kakehashi, Anna; Hagiwara, Akihiro; Imai, Norio; Nagano, Kasuke; Nishimaki, Fukumi; Banton, Marcy; Wei, Min; Fukushima, Shoji; Wanibuchi, Hideki

    2013-12-01

    To elucidate possible mode of action (MOA) and human relevance of hepatotumorigenicity in rats for ethyl tertiary-butyl ether (ETBE), male F344 rats were administered ETBE at doses of 0, 150 and 1000 mg/kg body weight twice a day by gavage for 1 and 2 weeks. For comparison, non-genotoxic carcinogen phenobarbital (PB) was applied at a dose of 500 ppm in diet. Significant increase of P450 total content and hydroxyl radical levels by low, high doses of ETBE and PB treatments at weeks 1 and 2, and 8-OHdG formation at week 2, accompanied accumulation of CYP2B1/2B2, CYP3A1/3A2 and CYP2C6, and downregulation of DNA oxoguanine glycosylase 1, induction of apoptosis and cell cycle arrest in hepatocytes, respectively. Up-regulation of CYP2E1 and CYP1A1 at weeks 1 and 2, and peroxisome proliferation at week 2 were found in high dose ETBE group. Results of proteome analysis predicted activation of upstream regulators of gene expression altered by ETBE including constitutive androstane receptor (CAR), pregnane-X-receptor (PXR) and peroxisome proliferator-activated receptors (PPARs). These results indicate that the MOA of ETBE hepatotumorigenicity in rats may be related to induction of oxidative stress, 8-OHdG formation, subsequent cell cycle arrest, and apoptosis, suggesting regenerative cell proliferation after week 2, predominantly via activation of CAR and PXR nuclear receptors by a mechanism similar to that of PB, and differentially by activation of PPARs. The MOA for ETBE hepatotumorigenicity in rats is unlikely to be relevant to humans.

  17. Comparison of methods for detecting mitomycin C- and ethyl nitrosourea-induced germ cell damage in mice: sperm enzyme activities, sperm motility, and testis weight

    SciTech Connect

    Ficsor, G.; Oldford, G.M.; Loughlin, K.R.; Panda, B.B.; Dubien, J.L.; Ginsberg, L.C.

    1984-01-01

    Testes weights, sperm motility and enzyme activities in single sperm were compared with respect to their ability to detect either developmental or mutational damage to germ cells. Male mice were injected i.p. with 2.5 mg/kg mitomycin C (MC) or 50 or 100 mg/kg ethylnitrosourea (ENU) or saline and were then killed at times such that sperm derived from treated vas sperm (SZ), spermatids (ST), preleptotene-late-spermatogonial cells (PLSG), spermatogonial cells (SG), or spermatogonial stem cells (SGS) could be evaluated. The authors conclude that testis weight, which is easily obtained, is a sensitive indicator of germ cell damage by these agents. Sperm from each animal were evaluated for sperm motility, acrosin activity, succinic dehydrogenase (SDH) activity with or without the competitive inhibitor malonate or after exposure to 60/sup 8/C for 10 min. The latter two assays were to detect sperm enzymes resistant to the inhibitor or heat. The presence of the acrosin protein was also detected immunologically. Of the sperm assays, acrosin activity proved to be the most sensitive indicator of germ cell damage and was the simplest to measure.

  18. Identification of an antioxidant, ethyl protocatechuate, in peanut seed testa.

    PubMed

    Huang, Shiow Chyn; Yen, Gow-Chin; Chang, Lee-Wen; Yen, Wen-Jye; Duh, Pin-Der

    2003-04-09

    The antioxidant activity and identification of the antioxidant component of peanut seed testa were investigated. The antioxidant activity of peanut seed testa was studied in the linoleic acid model system by using the ferric thiocyanate method. Among the five organic solvent extracts, the ethanolic extracts of peanut seed testa (EEPST) produced higher yields and stronger antioxidant activity than other organic solvent extracts. EEPST was separated into 17 fractions on silica gel column chromatography. Fraction 17, which showed the largest yield and significant antioxidant activity, was separated by thin-layer chromatography. Four major antioxidative subfractions were present. Subfraction 17-2 was found to be effective in preventing oxidation of linoleic acid. This subfraction was further fractionated and isolated and characterized by UV, MS, IR, and (1)H NMR techniques. The active compound was identified as ethyl protocatechuate (3,4-dihydroxybenzoic acid ethyl ester).

  19. Profile and antioxidant activity of phenolic extracts from 10 crabapples (Malus wild species).

    PubMed

    Li, Nan; Shi, Junling; Wang, Kun

    2014-01-22

    Phenolic products are highly demanded by the food and cosmetics industries and consumers due to their high antioxidant activities. To evaluate the potential of crabapples (Malus wild species) in preparing phenolic extracts, fruits of 10 crabapples grown in China were separately extracted with 80% (v/v) ethanol and ethyl acetate and the phenolic profiles, polyphenol (PC) and flavonoid contents (FC), and antioxidant activities of the extracts were analyzed. Chlorogenic acid, (-)-epicatechin, rutin, hyperin, and phlorizin appeared as the major phenolic compounds in all phenolic extracts. Ethanol extracts had PC of 302.83-1265.94 mg GAE/100g and FC of 352.45-2351.74 mg RE/100g, being 4.17 and 4.49 times those obtained in ethyl acetate extracts and much higher than those previously reported in apples. Malus wild species appeared as rich sources of phenolic compounds with high antioxidant activity, especially when high chlorogenic acid and rutin contents are emphasized.

  20. Phenolic content and antioxidant activity of Pereskia grandifolia Haw. (Cactaceae) extracts

    PubMed Central

    Sim, K. S.; Nurestri, A. M. Sri; Norhanom, A. W.

    2010-01-01

    The leaves of Pereskia grandifolia Haw. (Cactaceae), commonly known as “Jarum Tujuh Bilah” in Malaysia, have been traditionally used as natural remedy in folk medicine by the locals. In the present study, the antioxidant potential of P. grandifolia crude methanol and its fractionated extracts (hexane, ethyl acetate and water) have been investigated, employing three different established testing systems, such as scavenging activity on 1,1-diphenyl-2-picrylhydrazyl (DPPH) radicals, reducing power assay and β-carotene method. The total phenolic content of the P. grandifolia extracts was also assessed by the Folin-Ciocalteau’s method. The ethyl acetate extract showed significantly the highest total phenolic content, DPPH scavenging ability and antioxidant activity in β-carotene bleaching assay while the hexane extract possessed significantly strongest reducing power. The data obtained in these testing systems clearly establish the antioxidant potency of P. grandifolia. As such, this is the first report on the antioxidant activities of P. grandifolia. PMID:20931088

  1. Phytochemical and antimicrobial activities of the wild mango-Irvingia gabonensis extracts and fractions.

    PubMed

    Fadare, D A; Ajaiyeoba, E O

    2008-06-01

    Crude methanol extracts obtained from the leaf, stem bark and root of the wild mango, Irvingia gabonensis, were screened for antimicrobial properties by agar well diffusion method at three different concentrations (100 mg/ml, 50 mg/ml and 25 mg/ml) against six human pathogenic microorganisms consisting of four bacteria and two fungi. The hexane, chloroform, ethyl acetate and methanol fractions of the leaf and root methanol extracts were also subjected to the same assay at concentrations of 100 mg/ml-5mg/ml. Gentamicin and Tioconazole were used as positive and methanol as negative controls. Significant inhibitory activities were exhibited by the leaf and root extracts. The crude methanol extract of the root displayed the highest activity at a concentration of 100 mg/ml. It had a diameter of zone of inhibition of 19.7mm while the reference drug had 19.3mm on Pseudomonas aeruginosa, the most sensitive bacteria. The fungi used in this study were also very sensitive to the leaf extract. All the active extracts and fractions exhibited concentration-dependent activities against all the test organisms. Diameter of zones of inhibition ranges from 10.0-30.0 mm. The stem bark was inactive against all the studied organisms. The most active fraction was the ethyl acetate soluble fraction of the leaf which showed a comparable antimicrobial activity against the organisms at concentrations 100 mg/ml and 50 mg/ml comparable to the reference standard drug Gentamicin and Tioconazole. The ethyl acetate soluble fractions of leaf and root were found to show the highest activity. At a concentration of 5 mg/ml, the root ethyl acetate fraction inhibited the growth of all the bacteria tested. The phytochemical screening of the plant materials revealed the presence oftannins, saponins, alkaloids and anthraquinones and the absence of cardiac glycosides. Thin layer chromatography indicated the presence of phenolic compounds.

  2. Antibacterial Activity of Myristica fragrans against Oral Pathogens

    PubMed Central

    Shafiei, Zaleha; Shuhairi, Nadia Najwa; Md Fazly Shah Yap, Nordiyana; Harry Sibungkil, Carrie-Anne; Latip, Jalifah

    2012-01-01

    Myristica fragrans Houtt is mostly cultivated for spices in Penang Island, Malaysia. The ethyl acetate and ethanol extracts of flesh, mace and seed of Myristica fragrans was evaluated the bactericidal potential against three Gram-positive cariogenic bacteria (Streptococcus mutans ATCC 25175, Streptococcus mitis ATCC 6249, and Streptococcus salivarius ATCC 13419) and three Gram-negative periodontopathic bacteria (Aggregatibacter actinomycetemcomitans ATCC 29522, Porphyromonas gingivalis ATCC 33277, and Fusobacterium nucleatum ATCC 25586). Antibacterial activities of the extracts was determined by twofold serial microdilution, with minimum inhibitory concentrations (MIC) ranging from 1.25 to 640 mg/mL and 0.075 to 40 mg/mL. The minimum bactericidal concentration (MBC) was obtained by subculturing method. Among all extracts tested, ethyl acetate extract of flesh has the highest significant inhibitory effects against Gram-positive and Gram-negative bacteria with mean MIC value ranging from 0.625 to 1.25 ± 0.00 (SD) mg/mL; P = 0.017) and highest bactericidal effects at mean MBC value ranging from 0.625 mg/mL to 20 ± 0.00 (SD) mg/mL. While for seed and mace of Myristica fragrans, their ethanol extracts exhibited good antibacterial activity against both groups of test pathogens compared to its ethyl acetate extracts. All of the extracts of Myristica fragrans did not show any antibacterial activities against Fusobacterium nucleatum ATCC 25586. Thus, our study showed the potential effect of ethyl acetate and ethanol extracts from flesh, seed and mace of Myristica fragrans to be new natural agent that can be incorporated in oral care products. PMID:23049613

  3. Antibacterial Activity of Myristica fragrans against Oral Pathogens.

    PubMed

    Shafiei, Zaleha; Shuhairi, Nadia Najwa; Md Fazly Shah Yap, Nordiyana; Harry Sibungkil, Carrie-Anne; Latip, Jalifah

    2012-01-01

    Myristica fragrans Houtt is mostly cultivated for spices in Penang Island, Malaysia. The ethyl acetate and ethanol extracts of flesh, mace and seed of Myristica fragrans was evaluated the bactericidal potential against three Gram-positive cariogenic bacteria (Streptococcus mutans ATCC 25175, Streptococcus mitis ATCC 6249, and Streptococcus salivarius ATCC 13419) and three Gram-negative periodontopathic bacteria (Aggregatibacter actinomycetemcomitans ATCC 29522, Porphyromonas gingivalis ATCC 33277, and Fusobacterium nucleatum ATCC 25586). Antibacterial activities of the extracts was determined by twofold serial microdilution, with minimum inhibitory concentrations (MIC) ranging from 1.25 to 640 mg/mL and 0.075 to 40 mg/mL. The minimum bactericidal concentration (MBC) was obtained by subculturing method. Among all extracts tested, ethyl acetate extract of flesh has the highest significant inhibitory effects against Gram-positive and Gram-negative bacteria with mean MIC value ranging from 0.625 to 1.25 ± 0.00 (SD) mg/mL; P = 0.017) and highest bactericidal effects at mean MBC value ranging from 0.625 mg/mL to 20 ± 0.00 (SD) mg/mL. While for seed and mace of Myristica fragrans, their ethanol extracts exhibited good antibacterial activity against both groups of test pathogens compared to its ethyl acetate extracts. All of the extracts of Myristica fragrans did not show any antibacterial activities against Fusobacterium nucleatum ATCC 25586. Thus, our study showed the potential effect of ethyl acetate and ethanol extracts from flesh, seed and mace of Myristica fragrans to be new natural agent that can be incorporated in oral care products.

  4. Antioxidant and antibacterial activities on foodborne pathogens of Artocarpus heterophyllus Lam. (Moraceae) leaves extracts.

    PubMed

    Loizzo, M R; Tundis, R; Chandrika, U G; Abeysekera, A M; Menichini, F; Frega, N G

    2010-06-01

    Total water extract, ethyl acetate, and aqueous fractions from the leaves of Artocarpus heterophyllus were evaluated for phenolic content, antioxidant, and antibacterial activities against some foodborne pathogens such as E. coli, Listeria monocytogenes, Salmonella typhimurium, Salmonella enterica, Bacillus cereus, Enterococcus faecalis, and Staphylococcus aureus. The minimum inhibitory concentration (MICs) of extract and fractions determined by the agar dilution method were ranged from 221.9 microg/mL for ethyl acetate fraction to 488.1 microg/mL for total extract. In the agar diffusion method the diameters of inhibition were 12.2 for the total extract, 10.7 and 11.5 for ethyl acetate and aqueous fractions, respectively. A. heterophyllus showed significant antioxidant activity tested in different in vitro systems (DPPH, ABTS, FRAP, and Fe(2+) chelating activity assay). In particular, in DPPH assay A. heterophyllus total extract exhibited a strong antiradical activity with an IC(50) value of 73.5 microg/mL while aqueous fraction exerted the highest activity in FRAP assay (IC(50) value of 72.0 microg/mL). The total phenols content by Folin-Ciocalteau method was determined with the purpose of testing its relationship with the antioxidant and antibacterial activities.

  5. Anticariogenic activity and phytochemical studies of crude extract from some Indian plant leaves

    PubMed Central

    Barad, Mahesh K.; Ishnava, Kalpesh B.; Chauhan, Jenabhai B.

    2014-01-01

    Aim: The aim was to screen the selected Indian plants for their antibacterial efficacy against four cariogenic bacteria Lactobacillus acidophilus (LA)(Microbial Type Culture Collection [MTCC]-*447), Lactobacillus casei (LC) (MTCC-1423), Streptococcus mutans (SMU) (MTCC-890) and Staphylococcus aureus (MTCC-96). To identify and characterize active principle present in these plants for the treatment of dental caries. Materials and Methods: The dried plant leaves materials are extracted by cold extraction using hexane, ethyl acetate, methanol, and distilled water. The solvents were evaporated, and the dried masses were suspended in dimethyl sulfoxide and used for anticariogenic activity by agar well diffusion method. Minimum inhibitory concentration (MIC) was evaluated by two-fold serial broth dilution method. Preliminary phytochemical analysis of effective extract was carried out by thin-layer chromatography (TLC) and bioautography. Results: Ethyl acetate and hexane extract of Eucalyptus globules was found most effective against L. acidophilus with MIC value 31 μg/ml and 62 μg/ml, respectively. Ethyl acetate extracts of Acacia nilotica and methanolic extract of