WorldWideScience

Sample records for anti-infective activity screening

  1. Screening for potential anti-infective agents towards Burkholderia pseudomallei infection

    Science.gov (United States)

    Eng, Su Anne; Nathan, Sheila

    2014-09-01

    The established treatment for melioidosis is antibiotic therapy. However, a constant threat to this form of treatment is resistance development of the causative agent, Burkholderia pseudomallei, towards antibiotics. One option to circumvent this threat of antibiotic resistance is to search for new alternative anti-infectives which target the host innate immune system and/or bacterial virulence. In this study, 29 synthetic compounds were evaluated for their potential to increase the lifespan of an infected host. The nematode Caenorhabditis elegans was adopted as the infection model as its innate immune pathways are homologous to humans. Screens were performed in a liquid-based survival assay containing infected worms exposed to individual compounds and survival of untreated and compound-treated worms were compared. A primary screen identified nine synthetic compounds that extended the lifespan of B. pseudomallei-infected worms. Subsequently, a disc diffusion test was performed on these selected compounds to delineate compounds into those that enhanced the survival of worms via antimicrobial activity i.e. reducing the number of infecting bacteria, or into those that did not target pathogen viability. Out of the nine hits selected, two demonstrated antimicrobial effects on B. pseudomallei. Therefore, the findings from this study suggest that the other seven identified compounds are potential anti-infectives which could protect a host against B. pseudomallei infection without developing the risk of drug resistance.

  2. Screening for anti-infective properties of several medicinal plants of the Mauritians flora.

    Science.gov (United States)

    Rangasamy, Oumadevi; Raoelison, Guy; Rakotoniriana, Francisco E; Cheuk, Kiban; Urverg-Ratsimamanga, Suzanne; Quetin-Leclercq, Joelle; Gurib-Fakim, Ameenah; Subratty, Anwar Hussein

    2007-01-19

    Several plants of the Mauritian flora alleged to possess anti-infective properties were studied against different strains of pathogenic bacteria and fungi. The grounded dried plant materials were extracted with different extractants and screened for anti-microbial activity using the disk diffusion and the micro-dilution techniques. Preliminary screening revealed that the methanol extracts were most active. Salmonella enteritidis, Enterobacter cloacae and Bacillus subtilis were the three test organisms, which were found to be susceptible to all the crude methanolic extracts of the different plants investigated (100% susceptibility), followed by Escherichia coli (57.1%) and Pseudomonas aeruginosa (57.1%), and Staphylococcus aureus (28.6%). The lowest minimum inhibitory concentration recorded for the different crude methanol extracts against Staphylococcus aureus, Escherichia coli, Salmonella enteritidis, Enterobacter cloacae, Bacillus subtilis and the mould fungus Candida albicans were 500, 1000, 125, 250, 1000 and 125 micro g/ml, respectively. Bioautography using Cladosporium cucumerinum revealed that dichloromethane (DCM) extracts had the highest activity against the phytopathogenic fungus. It was also noted that the DCM extracts of Michelia champaca and Antidesma madagascariense yielded the maximum number of growth inhibiting compounds against Cladosporium cucumerinum. Activity of the different crude extracts was also investigated against several phytopathogenic filamentous fungi, Colletotrichum glocosporoides, Rhizoctonia solani, Sclerotinia sclerotium, Guignardia sp. and Fusarium oxysporum. It was found that crude hexane extracts as well as crude DCM extracts exhibited marked activity against several strains of fungi, especially Colletotrichum glocosporoides, Sclerotinia sclerotium and Guignardia sp. PMID:17011733

  3. The anti-infective activity of punicalagin against Salmonella enterica subsp. enterica serovar typhimurium in mice.

    Science.gov (United States)

    Li, Guanghui; Feng, Yuqing; Xu, Yunfeng; Wu, Qian; Han, Qi'an; Liang, Xiujun; Yang, Baowei; Wang, Xin; Xia, Xiaodong

    2015-07-01

    Punicalagin, a major bioactive component of pomegranate peel, has been proven to have antioxidant, antiviral, anti-apoptosis, and hepatoprotective properties. The aim of this study was to investigate the anti-infective activity of punicalagin in a mouse model. C57BL/6 mice were initially challenged with Salmonella enterica subsp. enterica serovar typhimurium (S. typhimurium) and then treated with punicalagin. Food and water consumption and body weight were recorded daily. On day 8 post infection, the mice were sacrificed to examine pathogen counts in tissues, hematological parameters, cytokine levels, and histological changes. Compared to mice only infected with S. typhimurium, punicalagin-treated mice had more food consumption and less weight loss. A higher survival rate and lower counts of viable S. typhimurium in feces, liver, spleen, and kidney were found in the punicalagin-treated mice. The enzyme linked immunosorbent assay showed that the levels of IL-6, IL-10, and IFN-γ in serum and the spleen and TNF-α in serum, the spleen and the liver were reduced by punicalagin. Moreover, more neutrophils and higher neutrophil-to-mononuclear cell ratios in the punicalagin-treated mice were observed. Histological examination showed that punicalagin protected cells in the liver and spleen from hemorrhagic necrosis. It is concluded that punicalagin has a beneficial effect against S. typhimurium infection in mice. The anti-infective properties, together with other nutritionally beneficial effects, make punicalagin a promising supplement in human food or animal feeds to prevent disease associated with S. typhimurium.

  4. Anti-infective Activity of 2-Cyano-3-Acrylamide Inhibitors with Improved Drug-Like Properties against Two Intracellular Pathogens.

    Science.gov (United States)

    Passalacqua, Karla D; Charbonneau, Marie-Eve; Donato, Nicholas J; Showalter, Hollis D; Sun, Duxin; Wen, Bo; He, Miao; Sun, Hanshi; O'Riordan, Mary X D; Wobus, Christiane E

    2016-07-01

    Due to the rise of antibiotic resistance and the small number of effective antiviral drugs, new approaches for treating infectious diseases are urgently needed. Identifying targets for host-based therapies represents an emerging strategy for drug discovery. The ubiquitin-proteasome system is a central mode of signaling in the eukaryotic cell and may be a promising target for therapies that bolster the host's ability to control infection. Deubiquitinase (DUB) enzymes are key regulators of the host inflammatory response, and we previously demonstrated that a selective DUB inhibitor and its derivative promote anti-infective activities in host cells. To find compounds with anti-infective efficacy but improved toxicity profiles, we tested a library of predominantly 2-cyano-3-acrylamide small-molecule DUB inhibitors for anti-infective activity in macrophages against two intracellular pathogens: murine norovirus (MNV) and Listeria monocytogenes We identified compound C6, which inhibited DUB activity in human and murine cells and reduced intracellular replication of both pathogens with minimal toxicity in cell culture. Treatment with C6 did not significantly affect the ability of macrophages to internalize virus, suggesting that the anti-infective activity interferes with postentry stages of the MNV life cycle. Metabolic stability and pharmacokinetic assays showed that C6 has a half-life in mouse liver microsomes of ∼20 min and has a half-life of approximately 4 h in mice when administered intravenously. Our results provide a framework for targeting the host ubiquitin system in the development of host-based therapies for infectious disease. Compound C6 represents a promising tool with which to elucidate the role of DUBs in the macrophage response to infection. PMID:27139470

  5. Anti-infective Natural Products from Cyanobacteria.

    Science.gov (United States)

    Niedermeyer, Timo Horst Johannes

    2015-10-01

    Cyanobacteria are a promising yet underexplored source for novel natural products with potent biological activities. While predominantly cytotoxic compounds have been isolated from cyanobacteria in the past, there are also a significant number of compounds known that possess anti-infective activities. As the need for novel anti-infective lead compounds is high, this manuscript aims at giving a concise overview on the current knowledge about anti-infective secondary metabolites isolated from cyanobacteria. Antibacterial, antifungal, antiviral, antiprotozoal, and molluscicidal activities are discussed. Covering up to February 2015.

  6. Anti-infective, cytotoxic and antioxidant activity of Ziziphus oxyphylla and Cedrela serrata

    Institute of Scientific and Technical Information of China (English)

    Rizwan Ahmad; Niyaz Ahmad; Atta Abbas Naqvi; Paul Cos; Louis Maes; Sandra Apers; Nina Hermans; Luc Pieters

    2016-01-01

    Objective: To search for the most active antimicrobial and antioxidant sub-fractions related to traditional use of Ziziphus oxyphylla (Z. oxyphylla) and Cedrela serrata (C. serrata) in Pakistan against infectious and liver diseases. Methods: Factions of different polarity were tested in vitro for their antiprotozoal, antimalarial, antibacterial and antifungal activity against different pathogens. Cytotoxicity on MRC-5 cell lines (human lung fibroblasts) as well as, in vitro radical scavenging activity was evaluated using the 1, 1-diphenyl-2-picrylhydrazyl radical assay. Results: The highest antiprotozoal activity was observed for the CHCl3 fractions of Z. oxyphylla roots and leaves, and C. serrata bark. The CHCl3 and EtOAc fractions of Z. oxyphylla roots, the CHCl3 fraction of Z. oxyphylla leaves, the EtOAc and the residual MeOH: H2O fraction of C. serrata bark showed antibacterial activity against Staphylo-coccus aureus. The same residual MeOH: H2O fraction of C. serrata bark was active against Candida albicans. The highest antioxidant activity was observed for the more hydrophilic EtOAc fractions of Z. oxyphylla leaves, C. serrata bark and leaves, and the residual MeOH:H2O fraction of C. serrata bark. Conclusions: This study supports at least in part the traditional uses of these plants for antimicrobial purposes and against liver diseases.

  7. Antimicrobial Activity of Lippia Species from the Brazilian Semiarid Region Traditionally Used as Antiseptic and Anti-Infective Agents

    Directory of Open Access Journals (Sweden)

    Cristiana da Purificação Pinto

    2013-01-01

    Full Text Available Lippia origanoides Kunth, Lippia alnifolia Schauer, and Lippia thymoides Martius and Schauer are shrubs used in the traditional Brazilian medicine as antiseptics, as well as in the treatment of infectious diseases. This study was designed to investigate the antibacterial and antifungal activities of the methanolic extracts of these species, as new potential sources of antimicrobial drugs. The antimicrobial activity of methanolic extracts was investigated against resistant yeasts and bacteria by agar disk diffusion. Then, the MIC determination of the most active species and its fractions in hexane, dichloromethane, ethyl acetate, and water was performed. By the agar diffusion assay, all species were active against at least two microorganisms, giving evidence to support their use in the popular medicine. L. origanoides leaves exhibited the widest antimicrobial action, inhibiting the growth of two Gram-positive bacteria and two yeasts; this activity was also confirmed by the MIC evaluation. The fractionation of L. origanoides crude extracts improved the activity in spectrum and intensity. The results obtained in this study indicate that L. origanoides may be a promising alternative in the treatment of bacterial and fungal infections and in the seeking of new antimicrobial drugs.

  8. Anti-infective potential of hot-spring bacteria

    Directory of Open Access Journals (Sweden)

    Pallavi Pednekar

    2011-01-01

    Full Text Available Aim and Background: Antibiotic resistance currently spans most of the known classes of natural and synthetic antibiotics; limiting our options for treatment of infections and demanding discovery of new classes of antibiotics. Much effort is being directed towards developing new antibiotics to overcome this problem. Success in getting novel chemical entities from microbial sources depends essentially on novelty of its habitat. The diversity of geographical location decides the type of micro-flora. In the past various terrestrial and aqueous microorganisms have provided several novel bioactive secondary metabolites of pharmaceutical importance. Hot-springs have not been as extensively exploited as other terrestrial resources. However, perseverance with such microbes augment the probability of getting novel bioactive compounds. Materials and Methods: Hot-springs soil samples were collected from Hot-springs in Maharashtra. Actinomycetes and other eubacteria were isolated from these soil samples by selective methods and purified. They were classified based on gram′s nature and morphology. Six representative morphological strains were screened for their anti-infective potential by agar well diffusion method as reported by Nathan P. et al (1974. The bioactivity of the active microbes was confirmed. Results: Seventy three strains of bacteria encompassing eight actinomycetes, and 65 eubacteria were isolated and purified. Among the actives eubacteria PPVWK106001 showed broad spectrum antibacterial activity encompassing both gram positive and gram negative bacterial test models. The extract was active against resistant bacteria such as MRSA and VREs. Activity was very specific as there was no activity against fungi even at 100 fold concentration. The active principle was extractable in butanol. Conclusions: The study showed that Hot-springs exhibit diverse bacteria and it serves as potential reservoirs for bacteria of antimicrobial importance with

  9. Anti-infective immunoadhesins from plants.

    Science.gov (United States)

    Wycoff, Keith; Maclean, James; Belle, Archana; Yu, Lloyd; Tran, Y; Roy, Chad; Hayden, Frederick

    2015-10-01

    Immunoadhesins are recombinant proteins that combine the ligand-binding region of a receptor or adhesion molecule with immunoglobulin constant domains. All FDA-approved immunoadhesins are designed to modulate the interaction of a human receptor with its normal ligand, such as Etanercept (Enbrel(®) ), which interferes with the binding of tumour necrosis factor (TNF) to the TNF-alpha receptor and is used to treat inflammatory diseases such as rheumatoid arthritis. Like antibodies, immunoadhesins have long circulating half-lives, are readily purified by affinity-based methods and have the avidity advantages conferred by bivalency. Immunoadhesins that incorporate normal cellular receptors for viruses or bacterial toxins hold great, but as yet unrealized, potential for treating infectious disease. As decoy receptors, immunoadhesins have potential advantages over pathogen-targeted monoclonal antibodies. Planet Biotechnology has specialized in developing anti-infective immunoadhesins using plant expression systems. An immunoadhesin incorporating the cellular receptor for anthrax toxin, CMG2, potently blocks toxin activity in vitro and protects animals against inhalational anthrax. An immunoadhesin based on the receptor for human rhinovirus, ICAM-1, potently blocks infection of human cells by one of the major causes of the common cold. An immunoadhesin targeting the MERS coronavirus is in an early stage of development. We describe here the unique challenges involved in designing and developing immunoadhesins targeting infectious diseases in the hope of inspiring further research into this promising class of drugs. PMID:26242703

  10. Anti-infective activities of Pelargonium sidoides (EPS® 7630): effects of induced NO production on Leishmania major in infected macrophages and antiviral effects as assessed in a fibroblast-virus protection assay.

    Science.gov (United States)

    Thäle, Carsten; Kiderlen, Albrecht Ferdinand; Kolodziej, Herbert

    2011-05-01

    EPs® 7630 is an aqueous-ethanolic extract of the roots of Pelargonium sidoides, employed in the treatment of upper respiratory tract infections. Its anti-infective activity is supposed to be associated with the activation of the nonspecific immune system. Using Leishmania major GFP-infected murine BMMΦ, the NO production of EPs® 7630-activated macrophages was correlated with the reduction of the GFP signal measured at single cell levels using flow cytometry. The anti-infectious effect of EPs® 7630 (3-10 µg/mL) on its own (NO production: 4-13 µM; signal reduction: 25-73 %) was less prominent than that in combination with IFN- γ (100 U/mL) (NO production: 20-27 µM; signal reduction: 35-78 %). Furthermore, supernatants of EPs® 7630-stimulated BMMΦ (10 µg/mL) significantly reduced the cytopathic effect of EMCV on L929 fibroblasts (antiviral activity 80 U/mL) when compared with an IFN- γ standard (100 U/mL). Direct addition of EPs® 7630 to L929 did not mediate cytoprotective effects. The antiviral components induced in BMMΦ by EPs® 7630 remain to be identified. Detection of any IFNs by ELISA was unsuccessful, which may be due to their very low concentrations in cell supernatants. The current data provide convincing support for the induction of anti-infectious responses by EPs® 7630.

  11. Preparation and Anti-Infective Activity of Houttuynia cordata Topical Cream%鱼腥草外用抗菌霜剂的制备及局部皮肤抗感染研究

    Institute of Scientific and Technical Information of China (English)

    梁菊; 陈姗; 刘秋伟; 池志娟

    2011-01-01

    以系统溶剂法分别制备了鱼腥草的石油醚提取物、氯仿提取物、乙酸乙酯提取物、正丁醇提取物和水提取物.各提取物的体外抑菌实验表明,鱼腥草的氯仿提取物对金黄色葡萄球菌、苏云金杆菌、大肠杆菌、枯草芽孢杆菌和白色葡萄球菌的生长具有很好的抑制作用.以该提取物为主要成分,制作了一种鱼腥草的外用抗菌霜剂.豚鼠皮肤刺激实验表明,该霜剂对皮肤无刺激性.豚鼠皮内注射金黄色葡萄球菌皮肤局部感染模型的建立及抗感染实验结果表明,该霜剂对金黄色葡萄球菌引起的皮肤局部感染有明显的治疗效果,每天给药3次,每次给药0.1 g(区域面积20 m%Five extracts of Houttuynia cordata was obtained using petroleum ether,chloroform,ethyl acetate,n-butanol and water as the solvents.The results of antibacterial experiments in vitro showed that chloroform fraction has strong antibacterial activity against Staphylococcus aureus,Bacillus thuringiensis,Escherichia coli,Bacillus subtilis,and Staphylococcus albus.A topical cream was prepared with chloroform extract as the main ingredient and was evaluated by acute skin irritancy in which the cream showed less irritant and safety for topical application.The guinea pig model of Staphylococcus aureus intradermal infection was then established and used for testing anti-infective activity of the cream.Skin redness and swelling disappeared after dermic administration 7 days with 0.1 g of the cream(20 mm×30 mm) three times a day.And the injected area has no bacteria survival by the bacterial culture of local skin in media.Those results hinted that Houttuynia cordata topical cream might be developed for potential clinical anti-infection drug.

  12. Screening and merger activity

    NARCIS (Netherlands)

    A. Banal-Estañol; P. Heidhues; R. Nitsche; J. Seldeslachts

    2010-01-01

    In our paper, the target of a proposed merger, by setting a reserve price, is able to screen prospective acquirers according to their (expected) ability to generate merger-specific synergies. Both empirical evidence and many merger models suggest that the difference between high and low-synergy merg

  13. Natural product inhibitors of fatty acid biosynthesis: synthesis of the marine microbial metabolites pseudopyronines A and B and evaluation of their anti-infective activities

    DEFF Research Database (Denmark)

    Giddens, Anna C.; Nielsen, Lone; Boshoff, Helena I.;

    2007-01-01

    Total syntheses of the title natural products, pseudopyronines A (1) and B (2), have been achieved using methyl β-oxo carboxylic ester starting materials. The natural products and a small set of structurally related compounds were evaluated for growth inhibitory activity against a range of pathog...

  14. Panax ginseng has anti-infective activity against opportunistic pathogen Pseudomonas aeruginosa by inhibiting quorum sensing, a bacterial communication process critical for establishing infection

    DEFF Research Database (Denmark)

    Song, Z; Kong, K F; Wu, H;

    2010-01-01

    immune systems and cystic fibrosis. The QS systems of P. aeruginosa use N-acylated homoserine lactone (AHL) as signal molecules. Previously we have demonstrated that Panax ginseng treatment allowed the animals with P. aeruginosa pneumonia to effectively clear the bacterial infection. We postulated......A and LasB and down-regulated the synthesis of the AHL molecules. Ginseng has a negative effect on the QS system of P. aeruginosa, may explain the ginseng-dependent bacterial clearance from the animal lungs in vivo in our previous animal study. It is possible that enhancing and repressing activities...... of ginseng are mutually exclusive as it is a complex mixture, as shown with the HPLC analysis of the hot water extract. Though ginseng is a promising natural synergetic remedy, it is important to isolate and evaluate the ginseng compounds associated with the anti-QS activity....

  15. Anti-infective activities of lactobacillus strains in the human intestinal microbiota: from probiotics to gastrointestinal anti-infectious biotherapeutic agents.

    Science.gov (United States)

    Liévin-Le Moal, Vanessa; Servin, Alain L

    2014-04-01

    A vast and diverse array of microbial species displaying great phylogenic, genomic, and metabolic diversity have colonized the gastrointestinal tract. Resident microbes play a beneficial role by regulating the intestinal immune system, stimulating the maturation of host tissues, and playing a variety of roles in nutrition and in host resistance to gastric and enteric bacterial pathogens. The mechanisms by which the resident microbial species combat gastrointestinal pathogens are complex and include competitive metabolic interactions and the production of antimicrobial molecules. The human intestinal microbiota is a source from which Lactobacillus probiotic strains have often been isolated. Only six probiotic Lactobacillus strains isolated from human intestinal microbiota, i.e., L. rhamnosus GG, L. casei Shirota YIT9029, L. casei DN-114 001, L. johnsonii NCC 533, L. acidophilus LB, and L. reuteri DSM 17938, have been well characterized with regard to their potential antimicrobial effects against the major gastric and enteric bacterial pathogens and rotavirus. In this review, we describe the current knowledge concerning the experimental antibacterial activities, including antibiotic-like and cell-regulating activities, and therapeutic effects demonstrated in well-conducted, placebo-controlled, randomized clinical trials of these probiotic Lactobacillus strains. What is known about the antimicrobial activities supported by the molecules secreted by such probiotic Lactobacillus strains suggests that they constitute a promising new source for the development of innovative anti-infectious agents that act luminally and intracellularly in the gastrointestinal tract.

  16. Automation of antimicrobial activity screening.

    Science.gov (United States)

    Forry, Samuel P; Madonna, Megan C; López-Pérez, Daneli; Lin, Nancy J; Pasco, Madeleine D

    2016-03-01

    Manual and automated methods were compared for routine screening of compounds for antimicrobial activity. Automation generally accelerated assays and required less user intervention while producing comparable results. Automated protocols were validated for planktonic, biofilm, and agar cultures of the oral microbe Streptococcus mutans that is commonly associated with tooth decay. Toxicity assays for the known antimicrobial compound cetylpyridinium chloride (CPC) were validated against planktonic, biofilm forming, and 24 h biofilm culture conditions, and several commonly reported toxicity/antimicrobial activity measures were evaluated: the 50 % inhibitory concentration (IC50), the minimum inhibitory concentration (MIC), and the minimum bactericidal concentration (MBC). Using automated methods, three halide salts of cetylpyridinium (CPC, CPB, CPI) were rapidly screened with no detectable effect of the counter ion on antimicrobial activity. PMID:26970766

  17. Anti-infective bovine colostrum oligosaccharides: Campylobacter jejuni as a case study.

    Science.gov (United States)

    Lane, Jonathan A; Mariño, Karina; Naughton, Julie; Kavanaugh, Devon; Clyne, Marguerite; Carrington, Stephen D; Hickey, Rita M

    2012-07-01

    Campylobacter jejuni is the leading cause of acute bacterial infectious diarrhea in humans. Unlike in humans, C. jejuni is a commensal within the avian host. Heavily colonized chickens often fail to display intestinal disease, and no cellular attachment or invasion has been demonstrated in-vivo. Recently, researchers have shown that the reason for the attenuation of C. jejuni virulence may be attributed to the presence of chicken intestinal mucus and more specifically chicken mucin. Since mucins are heavily glycosylated molecules this observation would suggest that glycan-based compounds may act as anti-infectives against C. jejuni. Considering this, we have investigated naturally sourced foods for potential anti-infective glycans. Bovine colostrum rich in neutral and acidic oligosaccharides has been identified as a potential source of anti-infective glycans. In this study, we tested oligosaccharides isolated and purified from the colostrum of Holstein Friesian cows for anti-infective activity against a highly invasive strain of C. jejuni. During our initial studies we structurally defined 37 bovine colostrum oligosaccharides (BCO) by HILIC-HPLC coupled with exoglycosidase digests and off-line mass spectroscopy, and demonstrated the ability of C. jejuni to bind to some of these structures, in-vitro. We also examined the effect of BCO on C. jejuni adhesion to, invasion of and translocation of HT-29 cells. BCO dramatically reduced the cellular invasion and translocation of C. jejuni, in a concentration dependent manner. Periodate treatment of the BCO prior to inhibition studies resulted in a loss of the anti-infective activity of the glycans suggesting a direct oligosaccharide-bacterial interaction. This was confirmed when the BCO completely prevented C. jejuni binding to chicken intestinal mucin, in-vitro. This study builds a strong case for the inclusion of oligosaccharides sourced from cow's milk in functional foods. However, it is only through further

  18. NEW ASPECTS OF ANTI-INFECTION IMMUNITY

    Directory of Open Access Journals (Sweden)

    E. P. Kisseleva

    2011-01-01

    Full Text Available Abstract. Four types of adaptive immune response which are regulated by different T-cell populations, namely Th1, Th2, Th17 and T regs have been described. At the first time classification is based on the difference in transcription factors but not due to diversity of cytokines produced. Each population of T-lymphocytes possesses a set of unique transcription factors and directions of cell signaling. Each type of immune responses plays a key role in the protection against certain types of pathogens. The Th1-response is important against intracellular bacteria and fungi, the Th17 — against extracellular, the Th2 — against yeasts and protozoa. T-regulatory cells control all types of immune responses. Diversity of immune response mechanisms occurs due to involvement of different effector cells. The Th1-type of response is connected with macrophage activation, Th2-cells cooperate with B-lymphocytes as well as attract eosinophils and mast cells. Th17 lymphocytes stimulate neutrophils and epithelial cells. T-cell differentiation is directed by the cytokines produced by innate immune cells. Phagocytes recognize molecular patterns at the surface of pathogens via pattern-recognition receptors (PRR, become activated and synthesize cytokines. Pathogen plays important role in this process while instructing dendritic cells. Pathogen dials a special code from a number of phagocyte surface receptors, which is named as «combinatory» recognition. Phagocytes possess several different types of activation and synthesize different cytokines that direct T-lymphocytes to a certain type of differentiation.

  19. SCREENING OF PLANTS FOR ANTI DERMATOPHYTE ACTIVITY

    Directory of Open Access Journals (Sweden)

    V.S. Chauhan, A. Suthar, V. Naik and K. Salkar*

    2012-05-01

    Full Text Available Mycotic infections of skin are caused by dermatophytes. Screening of plants for anti dermatophyte activity was carried out based on the literature search done. Native plants of Maharashtra (India were screened for anti dermatophyte activity. Various plant parts from different regions were collected and then extracted with three different solvents viz. alcohol, hydro-alcohol and aqueous. The obtained extracts were subjected for anti dermatophyte activity using agar-well diffusion technique. Three different concentrations of extract were checked for activity. Two species of dermatophytes, viz. - Trichophyton and Microsporum were used in the screening assay. Out of the twenty-eight plants screened by agar diffusion method, seven were found to be active with different activity profile. Methanol extract was the most active extract. Pterospermum suberifolium, Trachyspermum ammi, Peltaphorum pterocarpum, Ixora coccinia, Persicaria glabra, Terminallia elliptica and Cicca acida showed activity at different concentrations against the two species of dermatophytes. The data obtained can be used for further studying the anti dermatophyte potential of active plants.

  20. Identification of potential anti-infectives against Staphylococcus aureus using a Caenorhabditis elegans infection model

    Science.gov (United States)

    Kong, Cin; Rahman, Noorsaadah Abd; Nathan, Sheila

    2014-09-01

    The alarming increase of antibiotic-resistant Staphylococcus aureus and a delay in antibiotics development point to the need for novel therapeutic approaches to combat infection. To discover novel anti-infective agents, we screened a number of synthetic compounds comprising mainly of chalcone derivatives to explore their potential in promoting the survival of the nematode Caenorhabditis elegans upon infection by S. aureus. Screening of seven chalcone derivatives using both agar- and liquid-based assays revealed three positive hits that significantly prolonged the survival of S. aureus-infected nematodes. All the hits did not interfere with bacterial growth in vitro, proposing that the three compounds identified most probably act through mechanisms distinct from conventional antibiotics that target bacterial replication.

  1. Future potential for anti-infectives from bacteria - how to exploit biodiversity and genomic potential.

    Science.gov (United States)

    Müller, Rolf; Wink, Joachim

    2014-01-01

    The early stages of antibiotic development include the identification of novel hit compounds. Since actinomycetes and myxobacteria are still the most important natural sources of active metabolites, we provide an overview on these producers and discuss three of the most promising approaches toward finding novel anti-infectives from microorganisms. These are defined as the use of biodiversity to find novel producers, the variation of culture conditions and induction of silent genes, and the exploitation of the genomic potential of producers via "genome mining". Challenges that exist beyond compound discovery are outlined in the last section. PMID:24119567

  2. Study of the Active Screen Plasma Nitriding

    Institute of Scientific and Technical Information of China (English)

    Zhao Cheng; C. X. Li; H. Dong; T. Bell

    2004-01-01

    Active screen plasma nitriding (ASPN) is a novel nitriding process, which overcomes many of the practical problems associated with the conventional DC plasma nitriding (DCPN). Experimental results showed that the metallurgical characteristics and hardening effect of 722M24 steel nitrided by ASPN at both floating potential and anodic (zero) potential were similar to those nitrided by DCPN. XRD and high-resolution SEM analysis indicated that iron nitride particles with sizes in sub-micron scale were deposited on the specimen surface in AS plasma nitriding. These indicate that the neutral iron nitride particles, which are sputtered from the active screen and transferred through plasma to specimen surface, are considered to be the dominant nitrogen carder in ASPN. The OES results show that NH could not be a critical species in plasma nitriding.

  3. Solvothermal synthesis of ZnO nanoparticles and anti-infection application in vivo.

    Science.gov (United States)

    Bai, Xiangyang; Li, Linlin; Liu, Huiyu; Tan, Longfei; Liu, Tianlong; Meng, Xianwei

    2015-01-21

    Zinc oxide nanoparticles (ZnONPs) have been widely studied as the bacteriostatic reagents. However, synthesis of small ZnO nanoparticles with good monodispersion and stability in aqueous solution is still a challenge. Anti-infection research of ZnONPs used as antibacterial agent in vivo is rare. In this paper, a novel, sustainable, and simple method to synthesize ZnO nanoparticles with good monodispersion in aqueous low-temperature conditions and with a small molecule agent is reported. Inhibition zone test and the minimum inhibitory concentration test were performed to examine the antibacterial activity of ZnONPs against bacteria Staphylococcus aureus and Escherichia coli in vitro. For further application in vivo, low cytotoxicity and low acute toxicity in mice of ZnO were demonstrated. Finally, 4 nm ZnONPs combined with poly(vinyl alcohol) gel was used as antibacterial agent in rodent elytritis model, and significant anti-infection effect was proven. In one word, the present research would shed new light on the designing of antibacterial materials like ZnO with promising application in disinfection.

  4. A high-mobility group box 1 that binds to DNA, enhances pro-inflammatory activity, and acts as an anti-infection molecule in black rockfish, Sebastes schlegelii.

    Science.gov (United States)

    Xin-Peng, Zhao; Yong-Hua, Hu; Yong, Liu; Jing-Jing, Wang; Guang-Hua, Wang; Ren-Jie, Wang; Min, Zhang

    2016-09-01

    High-mobility group box (HMGB) 1 is a chromosomal protein that plays critical roles in DNA transcription, replication and repair. In addition, HMGB1 functions as a pro-inflammatory molecule in many vertebrates and invertebrates. In teleosts, very limited studies of HMGB1 have been reported. In this study, we identified a HMGB1 homologue (SsHMGB1) from black rockfish (Sebastes schlegelii) and analyzed its structure, expression and biological function. The open reading frame of SsHMGB1 is 621 bp, with a 5'-untranslated region (UTR) of 62 bp and a 3'-UTR of 645 bp. SsHMGB1 contains two typical HMG boxes and an acidic C-terminal tail. The deduced amino acid sequence of SsHMGB1 shares the highest overall identity (89.4%) with the HMGB1 of Anoplopoma fimbria. The expression of SsHMGB1 occurred in multiple tissues and was highest in the brain. Moreover, the mRNA level of SsHMGB1 in head kidney (HK) macrophages could be induced by Listonella anguillarum in a time-dependent manner. Recombinant SsHMGB1 purified from Escherichia coli (i) bound DNA fragments in a dose-dependent manner; and (ii) induced the expression of cytokines in HK macrophages, including a significant increase in TNF-α activity and enhanced mRNA level of TNF13B and IL-1 β, which are known to be involved in antibacterial defense; moreover, (iii) significantly improved the macrophage bactericidal activity together with reduced pathogen dissemination and replication of bacteria in fish kidney. These results indicated that SsHMGB1 is a novel HMGB1 that possesses apparent immunoregulatory properties and is likely to be involved in fighting bacterial infection. PMID:27492120

  5. Liposomes as novel anti-infectives targeting bacterial virulence factors?

    Science.gov (United States)

    Azeredo da Silveira, Samareh; Perez, Antonio

    2015-05-01

    A recent report commissioned by Prime Minister David Cameron and chaired by former Goldman Sachs chief economist Jim O'Neill warns that the emergence, persistence and spread of antimicrobial resistance could lead to 10 million deaths per year and cause an economic burden as much as US$100 trillion by 2050. In the midst of this global crisis, unprecedented paths are being explored to combat bacterial infection. Virulence factors, and more particularly pore-forming toxins, play a key role in increasing morbidity and mortality caused by drug-resistant bacterial infections. Novel anti-infective liposomes specifically targeting and neutralizing these cytotoxic toxins are potential game-changers in the fight against deadly infections. PMID:25850805

  6. Cytocompatibility with osteogenic cells and enhanced in vivo anti-infection potential of quaternized chitosan-loaded titania nanotubes.

    Science.gov (United States)

    Yang, Ying; Ao, Haiyong; Wang, Yugang; Lin, Wentao; Yang, Shengbing; Zhang, Shuhong; Yu, Zhifeng; Tang, Tingting

    2016-01-01

    Infection is one of the major causes of failure of orthopedic implants. Our previous study demonstrated that nanotube modification of the implant surface, together with nanotubes loaded with quaternized chitosan (hydroxypropyltrimethyl ammonium chloride chitosan, HACC), could effectively inhibit bacterial adherence and biofilm formation in vitro. Therefore, the aim of this study was to further investigate the in vitro cytocompatibility with osteogenic cells and the in vivo anti-infection activity of titanium implants with HACC-loaded nanotubes (NT-H). The titanium implant (Ti), nanotubes without polymer loading (NT), and nanotubes loaded with chitosan (NT-C) were fabricated and served as controls. Firstly, we evaluated the cytocompatibility of these specimens with human bone marrow-derived mesenchymal stem cells in vitro. The observation of cell attachment, proliferation, spreading, and viability in vitro showed that NT-H has improved osteogenic activity compared with Ti and NT-C. A prophylaxis rat model with implantation in the femoral medullary cavity and inoculation with methicillin-resistant Staphylococcus aureus was established and evaluated by radiographical, microbiological, and histopathological assessments. Our in vivo study demonstrated that NT-H coatings exhibited significant anti-infection capability compared with the Ti and NT-C groups. In conclusion, HACC-loaded nanotubes fabricated on a titanium substrate show good compatibility with osteogenic cells and enhanced anti-infection ability in vivo, providing a good foundation for clinical application to combat orthopedic implant-associated infections. PMID:27672479

  7. Anti-Infective Metabolites of a Newly Isolated Bacillus thuringiensis KL1 Associated with Kalmegh (Andrographis paniculata Nees.), a Traditional Medicinal Herb.

    Science.gov (United States)

    Roy, Sudipta; Yasmin, Sahana; Ghosh, Subhadeep; Bhattacharya, Somesankar; Banerjee, Debdulal

    2016-01-01

    This study was conducted to isolate endophytic bacteria possessing anti-infective property from Kalmegh (Andrographis paniculata Nees.), a well-known medicinal plant. A total of 23 strains were isolated from this plant among which the strain KL1, isolated from surface-sterilized leaf of this medicinal herb, showed broad-spectrum antagonism against an array of Gram-positive and -negative bacterial pathogens. Ethyl acetate extract of KL1-fermented media yielded a greenish amorphous substance retaining anti-infective property. Solvent-extracted crude material was separated by thin-layer chromatography, and the active ingredient was located by autobiogram analysis. The purified anti-infective compound was found as anthracene derivative as analyzed by ultraviolet and Fourier transform infrared spectroscopy. The strain was identified as Bacillus thuringiensis KL1 from cultural, physiochemical, and molecular aspects. The above results indicate the pharmaceutical potential of the candidate isolate. PMID:26997870

  8. Anti-Infective Metabolites of a Newly Isolated Bacillus thuringiensis KL1 Associated with Kalmegh (Andrographis paniculata Nees.), a Traditional Medicinal Herb.

    Science.gov (United States)

    Roy, Sudipta; Yasmin, Sahana; Ghosh, Subhadeep; Bhattacharya, Somesankar; Banerjee, Debdulal

    2016-01-01

    This study was conducted to isolate endophytic bacteria possessing anti-infective property from Kalmegh (Andrographis paniculata Nees.), a well-known medicinal plant. A total of 23 strains were isolated from this plant among which the strain KL1, isolated from surface-sterilized leaf of this medicinal herb, showed broad-spectrum antagonism against an array of Gram-positive and -negative bacterial pathogens. Ethyl acetate extract of KL1-fermented media yielded a greenish amorphous substance retaining anti-infective property. Solvent-extracted crude material was separated by thin-layer chromatography, and the active ingredient was located by autobiogram analysis. The purified anti-infective compound was found as anthracene derivative as analyzed by ultraviolet and Fourier transform infrared spectroscopy. The strain was identified as Bacillus thuringiensis KL1 from cultural, physiochemical, and molecular aspects. The above results indicate the pharmaceutical potential of the candidate isolate.

  9. Using antimicrobial host defense peptides as anti-infective and immunomodulatory agents.

    Science.gov (United States)

    Kruse, Thomas; Kristensen, Hans-Henrik

    2008-12-01

    Virtually all life forms express short antimicrobial cationic peptides as an important component of their innate immune defenses. They serve as endogenous antibiotics that are able to rapidly kill an unusually broad range of bacteria, fungi and viruses. Consequently, considerable efforts have been expended to exploit the therapeutic potential of these antimicrobial peptides. Within the last couple of years, it has become increasingly clear that many of these peptides, in addition to their direct antimicrobial activity, also have a wide range of functions in modulating both innate and adaptive immunity. For one class of antimicrobial peptides, such as the human defensins, their primary role may even be as immunomodulators. These properties potentially provide entirely new therapeutic approaches to anti-infective therapy.

  10. Active screening of magnetic field near power stations generator buses

    Directory of Open Access Journals (Sweden)

    B.I. Kuznetsov

    2013-12-01

    Full Text Available An experimental study technique for a prototyping system of active screening of power-frequency magnetic field distortions near power station generator buses via controllable magnetic field sources is presented. Results of experimental research on a proto-typing active screening system with different control algorithms are given.

  11. Associations between screen time and physical activity among Spanish adolescents.

    Directory of Open Access Journals (Sweden)

    Jose A Serrano-Sanchez

    Full Text Available BACKGROUND: Excessive time in front of a single or several screens could explain a displacement of physical activity. The present study aimed at determining whether screen-time is associated with a reduced level of moderate to vigorous physical activity (MVPA in Spanish adolescents living in favorable environmental conditions. METHODOLOGY/PRINCIPAL FINDINGS: A multi-stage stratified random sampling method was used to select 3503 adolescents (12-18 years old from the school population of Gran Canaria, Spain. MVPA, screen-time in front of television, computer, video game console and portable console was assessed in the classroom by fulfilling a standardized questionnaire. Bivariate and multivariate logistic regression analyses adjusted by a set of social-environmental variables were carried out. Forty-six percent of girls (95% CI±2.3% and 26% of boys (95% CI±2.1% did not meet the MVPA recommendations for adolescents. Major gender differences were observed in the time devoted to vigorous PA, video games and the total time spent on screen-based activities. Boys who reported 4 hours•week(-1 or more to total screen-time showed a 64% (OR = 0.61, 95% CI, 0.44-0.86 increased risk of failing to achieve the recommended adolescent MVPA level. Participation in organized physical activities and sports competitions were more strongly associated with MVPA than screen-related behaviors. CONCLUSIONS/SIGNIFICANCE: No single screen-related behavior explained the reduction of MVPA in adolescents. However, the total time accumulated through several screen-related behaviors was negatively associated with MVPA level in boys. This association could be due to lower availability of time for exercise as the time devoted to sedentary screen-time activities increases. Participation in organized physical activities seems to counteract the negative impact of excessive time in front of screens on physical activity.

  12. Screening of antioxidant activity in microalgae

    OpenAIRE

    Mariana F.G. Assunção; Sandrine da Ressurreição

    2014-01-01

    Due to the toxicity of synthetic antioxidants, the demand for alternative sources of antioxidants over the years has increased. The interest in such compounds is related to their importance in human health and food quality. Microalgae, a group of organisms with high morphological diversity and able to produce a wide variety of biochemical compounds are considered a promising, non expensive source of antioxidant compounds (Guedes et al., 2013a). This work reports the screening of several di...

  13. Effect of Winemaking on the Composition of Red Wine as a Source of Polyphenols for Anti-Infective Biomaterials

    Directory of Open Access Journals (Sweden)

    Arianna Di Lorenzo

    2016-04-01

    Full Text Available Biomaterials releasing bactericides have currently become tools for thwarting medical device-associated infections. The ideal anti-infective biomaterial must counteract infection while safeguarding eukaryotic cell integrity. Red wine is a widely consumed beverage to which many biological properties are ascribed, including protective effects against oral infections and related bone (osteoarthritis, osteomyelitis, periprosthetic joint infections and cardiovascular diseases. In this study, fifteen red wine samples derived from grapes native to the Oltrepò Pavese region (Italy, obtained from the winemaking processes of “Bonarda dell’Oltrepò Pavese” red wine, were analyzed alongside three samples obtained from marc pressing. Total polyphenol and monomeric anthocyanin contents were determined and metabolite profiling was conducted by means of a chromatographic analysis. Antibacterial activity of wine samples was evaluated against Streptococcus mutans, responsible for dental caries, Streptococcus salivarius, and Streptococcus pyogenes, two oral bacterial pathogens. Results highlighted the winemaking stages in which samples exhibit the highest content of polyphenols and the greatest antibacterial activity. Considering the global need for new weapons against bacterial infections and alternatives to conventional antibiotics, as well as the favorable bioactivities of polyphenols, results point to red wine as a source of antibacterial substances for developing new anti-infective biomaterials and coatings for biomedical devices.

  14. Screen Time and Physical Activity in Overweight and Obese Students

    Directory of Open Access Journals (Sweden)

    Hosseinzadeh

    2015-11-01

    Full Text Available Background One of the most important threats for children’s health status is being overweight and obesity, and related causes such as screen time prevalence. Prevalence of being overweight and obesity in children is associated with health risk consequences in adulthood. Objectives The purpose of this study was to assess the prevalence of screen time and physical activity in overweight and obese students. Patients and Methods In this cross sectional descriptive study we randomly selected 302 students, from all districts of Qazvin, who’s relative body mass index (RBMIs were above the 85th percentile. Their screen time and physical activity prevalence were assessed with two separate techniques (self-report and parent-report. Pearson correlation test and regression analysis were done to examine the association between RBMI, screen time and physical activity. Results Mean screen time in boys was more than girls, in both overweight screen time- self report technique (ST-SRT: 1.93 ± 0.24 vs. 1.26 ± 0.44, ST-PRT: 3.4 ± 0.22 vs. 2.1 ± 0.15 and obese subjects (ST-SRT: 1.88 ± 0.31 vs. 1.37 ± 0.49, ST-PRT: 3.2 ± 0.32 vs. 2.3 ± 0.34 yet overweight subjects had less total screen time than obese individuals (P < 0.05. Pearson correlations with one-tailed test indicated that screen time had a significant association with RBMI. In addition, there was a significant association between the two techniques of screen time and physical activity measurements. The model of regression for screen time and RBMI was significant (F = 45, P = 0.000, R2 = 0.42 and screen time explained about 16% of variance in RBMI (B = 0.021, SEB = 0.004, β = 0.325. Conclusions Our research determined an association between screen time, physical activity and RBMI. Screen time was a prominent predictor of RBMI in children. It is important for health workers to decrease screen time of children to prevent the prevalence of being overweight and obesity.

  15. Screen time, physical activity and depression risk in minority women

    OpenAIRE

    Jessica Y. Breland; Fox, Ashley M.; Horowitz, Carol R.

    2012-01-01

    Emerging research suggests that sedentary behavior, sometimes measured as screen time, may be an important correlate of depression. Physical activity, while not the direct opposite of sedentary behavior, has also been associated with depression (albeit inversely). Although low-income and minority populations may experience greater levels of depression, little research has focused on the relationships between screen time or physical activity and depression in low-income, minority populations i...

  16. Young Children's Screen Activities, Sweet Drink Consumption and Anthropometry

    DEFF Research Database (Denmark)

    Olafsdottir, Steingerdur; Ahrens, Wolfgang; Siani, Alfonso;

    2014-01-01

    Background/Objectives: This longitudinal study describes the relationship between young children’s screen time, dietary habits and anthropometric measures. The hypothesis was that television viewing and other screen activities at baseline result in increased consumption of sugar-sweetened beverages...... children, both on their consumption of sugary drinks and on an increase in BMI and central obesity. Our findings suggest that television viewing seems to have a stronger effect on food habits and anthropometry than other screen activities in this age group....

  17. Extract of Pelargonium sidoides (EPs 7630) displays anti-infective properties by enhanced phagocytosis and differential modulation of host-bacteria interactions.

    Science.gov (United States)

    Conrad, Andreas; Frank, Uwe

    2008-05-01

    EPs 7630 is an aqueous-ethanolic extract of the roots of PELARGONIUM SIDOIDES that displays well-documented benefits in the treatment of upper respiratory tract infections (URTI). IN VITRO and animal investigations have revealed various anti-infective properties of EPs 7630. The present review sums up recently published IN VITRO investigations that have shown positive effects on the activity of human peripheral blood phagocytes (PBP) and differential modulation of the interactions between group A streptococci and the host's epithelial barrier.

  18. High-Throughput Screening for Streptomyces Antibiotic Biosynthesis Activators

    OpenAIRE

    Li CHEN; Wang, Yemin; Guo, Hang; Xu, Min; Deng, Zixin; Tao, Meifeng

    2012-01-01

    A genomic cosmid library of Streptomyces clavuligerus was constructed and transferred efficiently by conjugation to Streptomyces lividans, and 12 distinct groups of overlapping cosmid clones that activated the silent actinorhodin biosynthesis gene cluster were identified. This generally applicable high-throughput screening procedure greatly facilitates the identification of antibiotic biosynthesis activators.

  19. Anti-infectives for systemic use prescribed in a Spanish hospital between 2009-2013.

    Science.gov (United States)

    March Rosselló, Gabriel Alberto; Mora, Arturo Artero; Pérez Rubio, Alberto; Eiros Bouza, José María

    2016-01-01

    The overuse and misuse of antimicrobials contribute to the emergence of antibiotic-resistant bacteria. The aim of this work was to analyse all the anti-infectives for systemic use (J ATC group) prescribed at the University Clinic Hospital of Valladolid (Spain) for the years 2009-2013. Amounts of anti-infectives (antibacterials, antifungals and antivirals) used in the period 2009-2013 were expressed as defined daily doses (DDDs) and as total expenditure, and the significance of the difference in consumption of anti-infectives and the relevant expenditure between years was evaluated from the overlapping of the corresponding confidence intervals at 95% confidence level of DDDs and expenditure. The results obtained showed that DDDs and expenditure of antibacterials decreased in the period 2009-2013. Antimycotics showed an upward trend in expenditure and DDDs in the five-year study period, but with major oscillations. The consumption of antivirals was practically constant in the period 2009-2011; in 2012, a significant reduction was observed and this reduction was conserved in 2013, although their expenditure increased year by year. In conclusion, in the period 2009-2013, expenditure on anti-infectives increased year to year. However, this increase in expenditure resulted in a downward trend of DDDs. PMID:27031892

  20. Preliminary study of anti-infective function of a copper-bearing stainless steel

    International Nuclear Information System (INIS)

    In this study the copper (Cu)-bearing stainless steel was developed to reduce the incidence of implant-associated infections in clinical areas. A 317L austenitic stainless steel containing 4.5% Cu (317L-Cu SS) was designed and fabricated, and its anti-infective function was preliminarily studied both in vitro and in vivo by means of antibacterial test, confocal laser scanning microscope (CLSM) and scanning electron microscopy (SEM) observations, and animal implantation. The results indicated that the 317L-Cu SS possessed strong antibacterial rates against both Escherichia coli and Staphylococcus aureus, and showed anti-infective ability by inhibiting the formation of bacterial bio-film on surface of the steel due to the release of Cu ions from the steel surface. The microbiological and histological evaluations from animal implantation further proved that the 317L-Cu SS could obviously reduce the happening of bacterial infection, and is potential to be used as a new class of surgical implant material with anti-infective function. - Highlights: ► 317L stainless steel containing 4.5% Cu (317L-Cu SS) showed strong antibacterial role. ► 317L-Cu SS could inhibit the formation of bacterial bio-film on its surface. ► 317L-Cu SS showed anti-infective role in vivo.

  1. LC-MS/MS for Therapeutic Drug Monitoring of anti-infective drugs

    NARCIS (Netherlands)

    Veringa, Anette; Sturkenboom, Marieke G.G.; Dekkers, Bart G.J.; Koster, Remco A.; Roberts, Jason A.; Peloquin, Charles A.; Touw, Daan J.; Alffenaar, Jan-Willem C.

    2016-01-01

    Therapeutic drug monitoring (TDM) is a tool used to integrate pharmacokinetic and pharmacodynamic knowledge to optimise and personalize drug therapy. TDM is of specific interest for anti-infectives: to assure adequate drug exposure and reduce adverse events, to increase patient compliance and to pre

  2. Substrate independent ATPase activity may complicate high throughput screening.

    Science.gov (United States)

    Tuntland, Micheal L; Fung, L W-M

    2016-10-01

    Inorganic phosphate release, [Pi], is often measured in an enzymatic reaction in a high throughput setting. Based on the published mechanism, we designed a protocol for our screening for inhibitors of SAICAR synthetase (PurC), and we found a gradual increase in [Pi] in positive control samples over the course of the day. Further investigation indicated that hydrolysis of ATP catalyzed by PurC, rather than substrate-related phosphate release, was responsible for a partial contribution to the signals in the control samples. Thus substrate-independent ATPase activity may complicate high throughput screening. PMID:27430931

  3. Diced electrophoresis gel assay for screening enzymes with specified activities.

    Science.gov (United States)

    Komatsu, Toru; Hanaoka, Kenjiro; Adibekian, Alexander; Yoshioka, Kentaro; Terai, Takuya; Ueno, Tasuku; Kawaguchi, Mitsuyasu; Cravatt, Benjamin F; Nagano, Tetsuo

    2013-04-24

    We have established the diced electrophoresis gel (DEG) assay as a proteome-wide screening tool to identify enzymes with activities of interest using turnover-based fluorescent substrates. The method utilizes the combination of native polyacrylamide gel electrophoresis (PAGE) with a multiwell-plate-based fluorometric assay to find protein spots with the specified activity. By developing fluorescent substrates that mimic the structure of neutrophil chemoattractants, we could identify enzymes involved in metabolic inactivation of the chemoattractants.

  4. Screening of Iranian plants for antifungal activity: Part 1

    Directory of Open Access Journals (Sweden)

    Amin Gh.R

    2002-07-01

    Full Text Available In this study, 250 species from 37 families of native Iranian plants were screened for in vitro antifungal activity against 19 fungal strains in vitro. Primarily, the crude extracts at concentration of 100μg/ml were tested. Of 250 extracts tested, 185(74% showed antifungal activity against at least one fungal strain. The outstanding species were Artemisia aucheri, Artemisia scoparia, Carthamus oxyacantha, Francoeuria undulate, Tripleurospermum disciform, and Xanthium spinosum.

  5. Recent advances in design of potential quinoxaline anti-infectives.

    Science.gov (United States)

    Jampilek, Josef

    2014-01-01

    Antimicrobial diazanaphthalenes are indispensable in the treatment of various infections. The quinoxaline scaffold possesses unique physicochemical properties and provides a possibility of a great number of targeted modifications. Quinoxaline-based compounds have a wide range of promising biological properties; therefore a special attention is paid to them for research and designing of new drugs. In fact, quinoxaline can be considered as a privileged structure. The scaffold can be easily and rapidly constructed, which emphasizes the significance of this favourable structure. The review is focused on recently reported potential antibacterial, antimycobacterial, antifungal and antiprotozoal agents derived from the quinoxaline scaffold, their mechanism of action and structure-activity relationships. A brief classification of synthetic pathways of quinoxaline derivatives is provided too.

  6. Screening strategies for active tuberculosis: focus on cost-effectiveness

    Science.gov (United States)

    Dobler, Claudia Caroline

    2016-01-01

    In recent years, there has been renewed interest in screening for active tuberculosis (TB), also called active case-finding (ACF), as a possible means to achieve control of the global TB epidemic. ACF aims to increase the detection of TB, in order to diagnose and treat patients with TB earlier than if they had been diagnosed and treated only at the time when they sought health care because of symptoms. This will reduce or avoid secondary transmission of TB to other people, with the long-term goal of reducing the incidence of TB. Here, the history of screening for active TB, current screening practices, and the role of TB-diagnostic tools are summarized and the literature on cost-effectiveness of screening for active TB reviewed. Cost-effectiveness analyses indicate that community-wide ACF can be cost-effective in settings with a high incidence of TB. ACF among close TB contacts is cost-effective in settings with a low as well as a high incidence of TB. The evidence for cost-effectiveness of screening among HIV-infected persons is not as strong as for TB contacts, but the reviewed studies suggest that the intervention can be cost-effective depending on the background prevalence of TB and test volume. None of the cost-effectiveness analyses were informed by data from randomized controlled trials. As the results of randomized controlled trials evaluating different ACF strategies will become available in future, we will hopefully gain a better understanding of the role that ACF can play in achieving global TB control. PMID:27418848

  7. Phytochemical Screening and Evaluation of Analgesic Activity of Oroxylum indicum

    Science.gov (United States)

    Das, B. K.; Al-Amin, M. M.; Russel, S. M.; Kabir, S.; Bhattacherjee, R.; Hannan, J. M. A.

    2014-01-01

    We aimed to study phytochemical screening and analgesic activity of ethanol extract of Oroxylum indicum. The dried powder of the barks of the plant was extracted with 95% ethanol and was subjected to various phytochemical tests to ascertain the principle constituents contained in the extract. The result revealed the presence of alkaloids, flavonoids, tannins, glycosides in the ethanol extract of Oroxylum indicum. The extract was screened for analgesic activity by using hot plate, acetic acid-induced writhing and formalin test. The ethanol extract of the plant at two different doses (250 and 500 mg/kg) showed significant (Pflavonoids and tannins might be responsible for the analgesic activity. We suggest that ethanol extract of Oroxylum indicum might have potential chemical constituents that could be used in the future for the development of novel analgesic agent. PMID:25593396

  8. Screening for lipase activity in the oil palm.

    Science.gov (United States)

    Sambanthamurthi, R; Rajanaidu, N; Hasnah Parman, S

    2000-12-01

    The oil palm mesocarp contains an endogenous lipase which is strongly activated at low temperature. Lipase activity is thus very conveniently assayed by prior exposure of the fruits to low temperature. More than 100 oil palm samples from the germplasm collection of the Palm Oil Research Institute of Malaysia (now known as the Malaysian Palm Oil Board) were screened for non-esterified fatty acid activity using both the low-temperature activation assay and a radioactivity assay. The results showed good correlation between assay procedures. The different samples had a very wide range of lipase activity. Elaeis oleifera samples had significantly lower lipase activity compared with E. guineensis (var. tenera) samples. Even within E. guineensis (var. tenera), there was a wide range of activity. The results confirmed that lipase activity is genotype-dependent. Selection for lipase genotypes is thus possible and this will have obvious commercial value. PMID:11171201

  9. Marine-Derived Metabolites of S-Adenosylmethionine as Templates for New Anti-Infectives

    Directory of Open Access Journals (Sweden)

    Janice R. Sufrin

    2009-08-01

    Full Text Available S-Adenosylmethionine (AdoMet is a key biochemical co-factor whose proximate metabolites include methylated macromolecules (e.g., nucleic acids, proteins, phospholipids, methylated small molecules (e.g., sterols, biogenic amines, polyamines (e.g., spermidine, spermine, ethylene, and N-acyl-homoserine lactones. Marine organisms produce numerous AdoMet metabolites whose novel structures can be regarded as lead compounds for anti-infective drug design.

  10. Causes and consequences of anti-infective drug stock-outs.

    Science.gov (United States)

    Luans, C; Cardiet, I; Rogé, P; Baslé, B; Le Corre, P; Revest, M; Michelet, C; Tattevin, P

    2014-10-01

    Anti-infective drugs stock-outs are increasingly frequent, and this is unlikely to change. There are numerous causes for this, mostly related to parameters difficult to control: i) 60 to 80% of raw material or components are produced outside of Europe (compared to 20% 30 years ago), with subsequent loss of independence for their procurement; ii) the economic crisis drives the pharmaceutical companies to stop producing drugs of limited profitability (even among important drugs); iii) the enforcement of regulatory requirements and quality control procedures result in an increasing number of drugs being blocked during production. The therapeutic class most affected by drug stock-outs is that of anti-infective drugs, especially injectable ones, and many therapeutic dead ends have recently occurred. We provide an update on this issue, and suggest 2 major actions for improvement: i) to implement a group dedicated to anticipating drug stock-outs within the anti-infective committee in each health care center, with the objectives of organizing and coordinating the response whenever a drug stock-out is deemed at risk (i.e., contingency plans, substitution, communication to prescribers); ii) a national reflection lead by scientific societies, in collaboration with government agencies, upstream of the most problematic drug stock-outs, to elaborate and disseminate consensus guidelines for the management of these stock-outs.

  11. Screening marine organisms for antimicrobial activity against clinical pathogens

    Digital Repository Service at National Institute of Oceanography (India)

    PrabhaDevi; Wahidullah, S.; Tonima, K.; DeSouza, L.

    extracts of forty marine organisms belonging to different phyla and fractions of active extracts were screened for their antimicrobial effects on human pathogens. A broad panel of microbial pathogens associated with various skin infections, urinary... aeruginosa B2 Gram Negative Urinary tract infection 3. Staphylococcus aureus B3 Gram Positive Skin infection 4. Salmonella typhi (i) B4 Gram Negative Typhoid 5. Shigella flexineri B5 Gram Negative Gastrointestin al infection 6. Klebsiella sp. B6 Gram...

  12. Development and Validation of a Novel Leishmania donovani Screening Cascade for High-Throughput Screening Using a Novel Axenic Assay with High Predictivity of Leishmanicidal Intracellular Activity

    Science.gov (United States)

    Nühs, Andrea; De Rycker, Manu; Manthri, Sujatha; Comer, Eamon; Scherer, Christina A.; Schreiber, Stuart L.; Ioset, Jean-Robert; Gray, David W.

    2015-01-01

    Visceral leishmaniasis is an important parasitic disease of the developing world with a limited arsenal of drugs available for treatment. The existing drugs have significant deficiencies so there is an urgent need for new and improved drugs. In the human host, Leishmania are obligate intracellular parasites which poses particular challenges in terms of drug discovery. To achieve sufficient throughput and robustness, free-living parasites are often used in primary screening assays as a surrogate for the more complex intracellular assays. We and others have found that such axenic assays have a high false positive rate relative to the intracellular assays, and that this limits their usefulness as a primary platform for screening of large compound collections. While many different reasons could lie behind the poor translation from axenic parasite to intracellular parasite, we show here that a key factor is the identification of growth slowing and cytostatic compounds by axenic assays in addition to the more desirable cytocidal compounds. We present a screening cascade based on a novel cytocidal-only axenic amastigote assay, developed by increasing starting density of cells and lowering the limit of detection, and show that it has a much improved translation to the intracellular assay. We propose that this assay is an improved primary platform in a new Leishmania screening cascade designed for the screening of large compound collections. This cascade was employed to screen a diversity-oriented-synthesis library, and yielded two novel antileishmanial chemotypes. The approach we have taken may have broad relevance to anti-infective and anti-parasitic drug discovery. PMID:26407168

  13. Development and Validation of a Novel Leishmania donovani Screening Cascade for High-Throughput Screening Using a Novel Axenic Assay with High Predictivity of Leishmanicidal Intracellular Activity.

    Science.gov (United States)

    Nühs, Andrea; De Rycker, Manu; Manthri, Sujatha; Comer, Eamon; Scherer, Christina A; Schreiber, Stuart L; Ioset, Jean-Robert; Gray, David W

    2015-09-01

    Visceral leishmaniasis is an important parasitic disease of the developing world with a limited arsenal of drugs available for treatment. The existing drugs have significant deficiencies so there is an urgent need for new and improved drugs. In the human host, Leishmania are obligate intracellular parasites which poses particular challenges in terms of drug discovery. To achieve sufficient throughput and robustness, free-living parasites are often used in primary screening assays as a surrogate for the more complex intracellular assays. We and others have found that such axenic assays have a high false positive rate relative to the intracellular assays, and that this limits their usefulness as a primary platform for screening of large compound collections. While many different reasons could lie behind the poor translation from axenic parasite to intracellular parasite, we show here that a key factor is the identification of growth slowing and cytostatic compounds by axenic assays in addition to the more desirable cytocidal compounds. We present a screening cascade based on a novel cytocidal-only axenic amastigote assay, developed by increasing starting density of cells and lowering the limit of detection, and show that it has a much improved translation to the intracellular assay. We propose that this assay is an improved primary platform in a new Leishmania screening cascade designed for the screening of large compound collections. This cascade was employed to screen a diversity-oriented-synthesis library, and yielded two novel antileishmanial chemotypes. The approach we have taken may have broad relevance to anti-infective and anti-parasitic drug discovery. PMID:26407168

  14. Development and Validation of a Novel Leishmania donovani Screening Cascade for High-Throughput Screening Using a Novel Axenic Assay with High Predictivity of Leishmanicidal Intracellular Activity.

    Directory of Open Access Journals (Sweden)

    Andrea Nühs

    2015-09-01

    Full Text Available Visceral leishmaniasis is an important parasitic disease of the developing world with a limited arsenal of drugs available for treatment. The existing drugs have significant deficiencies so there is an urgent need for new and improved drugs. In the human host, Leishmania are obligate intracellular parasites which poses particular challenges in terms of drug discovery. To achieve sufficient throughput and robustness, free-living parasites are often used in primary screening assays as a surrogate for the more complex intracellular assays. We and others have found that such axenic assays have a high false positive rate relative to the intracellular assays, and that this limits their usefulness as a primary platform for screening of large compound collections. While many different reasons could lie behind the poor translation from axenic parasite to intracellular parasite, we show here that a key factor is the identification of growth slowing and cytostatic compounds by axenic assays in addition to the more desirable cytocidal compounds. We present a screening cascade based on a novel cytocidal-only axenic amastigote assay, developed by increasing starting density of cells and lowering the limit of detection, and show that it has a much improved translation to the intracellular assay. We propose that this assay is an improved primary platform in a new Leishmania screening cascade designed for the screening of large compound collections. This cascade was employed to screen a diversity-oriented-synthesis library, and yielded two novel antileishmanial chemotypes. The approach we have taken may have broad relevance to anti-infective and anti-parasitic drug discovery.

  15. Polyherbal preparation for anti-diabetic activity: A screening study

    OpenAIRE

    Noopur Srivastava; Gaurav Tiwari; Ruchi Tiwari

    2010-01-01

    Objective: To screen the Polyherbal preparation for anti-diabetic activity in rats. Materials and Methods: The blood glucose lowering activity of the Polyherbal preparation-I (1:1:1 of Wheat germ oil, Coriandrum sativum and Aloe vera) was studied in normal rats after oral administration at doses of 1.0 and 2.0 ml/kg and Polyherbal preparation-I, II (Wheat germ oil, fresh juice of C. sativum and Aloe vera in the ratio of 2:2:1), and III (Wheat germ oil, fresh juice of C. sativum and Aloe vera ...

  16. Phytochemical Screening and Antidiarrhoeal Activity of Hyptis suaveolens

    Directory of Open Access Journals (Sweden)

    Md. Zeshan Hashib Shaikat

    2012-08-01

    Full Text Available Summary. Hyptis suaveolens leaf has been used in conventional therapies for various disease conditions, including diarrhea. However, some of the therapeutic potentials of the plant have not been scientifically evaluated. Hence, the present study was aimed to evaluate the antidiarrhoeal activity of ethanol extract of Hyptis suaveolens leaf against an experimental model of castor oil-induced diarrhea in mice. Phytochemical screening of the plant extracts for their active constituents was also performed following standard procedures. Oral administration of the said ethanol extract (250 and 500 mg/kg showed significant (P<0.01 and dose-dependent inhibitory activity against castor oil induced diarrhoea. The onset of diarrhoea induced by castor oil was significantly delayed by administration of the plant extract. The results were comparable to those of standard antimotility drug, loperamide (50 mg/kg. Preliminary phytochemical screening shows the presence of alkaloid, glycoside, saponin, tannin and flavonoid as major constituents. The results indicate the presence of some active principles in the plant extract possessing anti-diarrhoeal effect and justify its traditional use in the treatment for diarrhoea. Industrial relevance. Diarrheal diseases pose a leading cause of morbidity and mortality worldwide.  Moreover, in developing countries, the cost of modern synthetic medicines is out of reach of the common man, especially those in rural areas. A large population of the Indian subcontinent depend on traditional system of medicine for their physical and psychological health needs. Hence there is an intensive search for natural products which are biologically active against diarrhea. In this study, the antidiarrhoeal activity of H S. was studied and the results revealed that the ethanol leaf extract of Hyptis suaveolens extracts significantly reduced induction time of diarrhoea and  number of diarrhoeal episodes in the orally treated mice. The results

  17. Application Of Active Screen Method For Ion Nitriding Efficiency Improvement

    Directory of Open Access Journals (Sweden)

    Ogórek M.

    2015-06-01

    Full Text Available Paper presents the research of austenitic steel AISI 304 after ion nitriding at 400°C and at t =4h, for the two different variants of samples distribution in the working plasma reactive chamber tube. In order to assess the effectiveness of ion nitriding variants emission spectroscopy – GDOES, surface hardness tests, microstructure research (LM of nitrided layers were made. It has been found that the use of active screens increases the surface layer thickness and depth of nitrogen diffusion into austenitic steel 304.

  18. Screening of some Nigerian plants for molluscicidal activity.

    Science.gov (United States)

    Kela, S L; Ogunsusi, R A; Ogbogu, V C; Nwude, N

    1989-01-01

    Methanolic (MEOH), evaporated crude water (ECW) and unevaporated crude water (UECW) extracts of 25 Nigerian plants, used for different medicinal and domestic purposes were screened for molluscacidal activity on laboratory-reared Lymnaea natalensis Krauss. Seven of the plants were not active; extracts from 18 (72 per cent) of the plants, some of which are renowned fish poisons, had molluscicidal activity. These were Acacia nilotica, Aristolochia albida, Balanites aegyptiaca, Blighia sapida, Boswellia dalzielii, Detarium microcarpum, Gnidia kraussiana, Kigelia africana, Nauclea latifolia, Opilia celtidefolia, Parkia clappertoniana, Polygonum limbatum, Pseudocedrela kotschyi, Sclerocarya birrea, Securidaca longipedunculata, Ximenia americana, Vetiveria nigritana and Ziziphus abyssinica. The LC50 of these extracts were determined. It is strongly recommended that the toxic effects of these extracts against fish, cercariae, snail eggs and mammals be further investigated so as to determine the right concentration, especially for use in fish ponds. PMID:2626572

  19. Mining Chemical Activity Status from High-Throughput Screening Assays

    KAUST Repository

    Soufan, Othman

    2015-12-14

    High-throughput screening (HTS) experiments provide a valuable resource that reports biological activity of numerous chemical compounds relative to their molecular targets. Building computational models that accurately predict such activity status (active vs. inactive) in specific assays is a challenging task given the large volume of data and frequently small proportion of active compounds relative to the inactive ones. We developed a method, DRAMOTE, to predict activity status of chemical compounds in HTP activity assays. For a class of HTP assays, our method achieves considerably better results than the current state-of-the-art-solutions. We achieved this by modification of a minority oversampling technique. To demonstrate that DRAMOTE is performing better than the other methods, we performed a comprehensive comparison analysis with several other methods and evaluated them on data from 11 PubChem assays through 1,350 experiments that involved approximately 500,000 interactions between chemicals and their target proteins. As an example of potential use, we applied DRAMOTE to develop robust models for predicting FDA approved drugs that have high probability to interact with the thyroid stimulating hormone receptor (TSHR) in humans. Our findings are further partially and indirectly supported by 3D docking results and literature information. The results based on approximately 500,000 interactions suggest that DRAMOTE has performed the best and that it can be used for developing robust virtual screening models. The datasets and implementation of all solutions are available as a MATLAB toolbox online at www.cbrc.kaust.edu.sa/dramote and can be found on Figshare.

  20. Screening of Antibacterial Activities of Marine Gastropod Hemifusus Pugilinus

    Directory of Open Access Journals (Sweden)

    S. Sugesh

    2013-01-01

    Full Text Available In the present investigation was carried out to screen the antibacterial activities of marine gastropod Hemifusus pugilinus. The whole body of the animal was extracted in three different solvents such as, ethanol, methanol and water. The antibacterial properties were studied using 10 human pathogenic microorganisms such as, Escherichia coli, Klebsiella oxytoca, K. pnuemoniae, Lactobacillus vulgaris, Proteus mirabilis, Pseudomonas aeruginosa, Salmonella typhi, S. paratyphi, Staphylococcus aureus, and Vibrio paraheamolyticus. The ethanolic extracts of H. pugilinus showed maximum antibacterial activities against E. coli (8 mm and minimum activities against Vibrio paraheamolyticus (2 mm, Methanolic extracts showed highest activity in E. coli (6 mm and lowest activity against S. paratyphi (1 mm and the extract of water showed antibacterial activities against E. coli K. oxytoca and S. paratyphi. The crude extracts were purified in silica gel column chromatography with 11 fractions. In that E:M, 16:4, 12:8, 10:10, which showed maximum zone of inhibition against E.coli (4 mm, K. oxytoca (4 mm, K. pneumoniae (3 mm, L. vulgaris (4 mm and V. parahemolyticus (5 mm. 18:2, 8:12, 6:14, 4:12 and 2:18 with these fractions showed minimum activities against the all pathogenic microbial forms.

  1. Performance on the Functional Movement Screen in older active adults

    Institute of Scientific and Technical Information of China (English)

    Ulrike H. Mitchell; A. Wayne Johnson; Pat R. Vehrs; J. Brent Feland; Sterling C. Hilton

    2016-01-01

    Background: The Functional Movement Screen (FMS™) has become increasingly popular for identifying functional limitations in basic functional movements. This exploratory and descriptive study was undertaken to confirm feasibility of performing the FMS™ in older active adults, assess prevalence of asymmetries and to evaluate the relationship between functional movement ability, age, physical activity levels and body mass index (BMI). Methods: This is an observational study;97 men (n=53) and women (n=44) between the ages of 52 and 83 participated. BMI was computed and self-reported physical activity levels were obtained. Subjects were grouped by age (5-year intervals), BMI (normal, over-weight, and obese) and sex. Each participant’s performance on the FMS™was digitally recorded for later analysis. Results: The youngest age group (50–54 years) scored highest in all seven tests and the oldest age group (75+) scored lowest in most of the tests compared to all other age groups. The subjects in the“normal weight”group performed no different than those who were in the“overweight”group;both groups performed better than the“obese”group. Of the 97 participants 54 had at least one asymmetry. The pairwise correlations between the total FMS™score and age (r=−0.531), BMI (r=−0.270), and the measure of activity level (r=0.287) were significant (p<0.01 for all). Conclusion: FMS™scores decline with increased BMI, increased age, and decreased activity level. The screen identifies range of motion-and strength-related asymmetries. The FMS™can be used to assess functional limitations and asymmetries. Future research should evaluate if a higher total FMS™score is related to fewer falls or injuries in the older population.

  2. Chinese patent of anti-infective urinary catheter%抗感染尿管获中国专利现况

    Institute of Scientific and Technical Information of China (English)

    熊国兵; 王寓; 邱明星

    2015-01-01

    application. METHODS:Al related Chinese patent papers of anti-infective urinary catheters were retrieved by Google’s proprietary search platform (http://www.google.com/advanced_patent_search) until the deadline of March 26, 2014, with the search strategy of‘Return the patents with the fol owing proprietary name:urinary catheter’. RESULTS AND CONCLUSION:According to the predefined search strategy, 949 potential y relevant patent papers were screened out for further identification, and 23 papers referred to anti-infective catheters that were obviously eligible were included. The analyses showed that:(1) The antibacterial coating agents of the majority of papers were antibacterial agents of nano-inorganic metal cations, only four papers used antibiotic coated. (2) The drug-eluting catheters were mainly composite-coated. (3) The drug release modes from coating were mainly extended-release but release mechanism was not clarified. (4) The preparation process was chemical bond or ionic bond in one paper, blending methods in one paper, repeated electroplating in one paper, electrospinning technology in one paper, and physical impregnation methods in 12 papers (52.17%). (5) The antimicrobial mode was ultrasonic-antibacterial method in two patent papers, sterile sleeve in one paper, hydrophilic coating in one paper, catheter made by blending polymer material and anti-infective agents in one paper, drug coated films made by coating with antimicrobial drug liquid and drying process in 20 papers (82.61%). In conclusion, there have been no translational and applied clinical researches about the anti-infective urinary catheter, and the relevant researches were only at the laboratory level. The research methods of Chinese patent for anti-infective urinary catheter were limited, and need to be further improved.

  3. Phytochemical screening and antioxidant activity of Lebanese Eryngium creticum L.

    Institute of Scientific and Technical Information of China (English)

    Hussein Farhan; Fatima Malli; Hassan Rammal; Akram Hijazi; Ali Bassal; Nawal Ajouz; Bassam Badran

    2012-01-01

    Objective: To determine the phytochemical screening and quantification of total phenolics contents in fresh Eryngium creticum (E. creticum) leaves and stems extract and to evaluate its total antioxidant activity. Methods: Quantification of total phenolics contents in fresh E. creticum leaves and stems extract and evaluation of its total antioxidant activity, were done using the spectrophotometric analyses. Results: The consumption of 100 g of fresh E. creticum leaves and stems could provide antioxidants equivalent to (78.50±0.80) mg of vitamin C and (50.42±0.50) mg of vitamin C, respectively. Conclusions: From this study, it can be concluded that E. creticum can be interesting to prevent diseases directly linked to oxidative stress.

  4. Medical Screening for Individuals Supporting Spacecraft Launch and Landing Activities in Remote Locations

    Science.gov (United States)

    Powers. W. Edward

    2010-01-01

    This viewgraph presentation reviews the medical screening process and spacecraft launch and landing mission activities for astronauts. The topics include: 1) Launch and Landing Mission Overview; 2) Available Resources; and 3) Medical Screening Process.

  5. Screening and antibacterial activity analysis of some important medicinal plants

    Directory of Open Access Journals (Sweden)

    G. Senthilmurugan Viji

    2013-02-01

    Full Text Available The screening and study of five different plant specimens belonging to different families for phytochemical constituents was performed using generally accepted laboratory technique for qualitative determinations. The constituents screened were saponins, combined anthraquinones, terpenoids, flavonoids, carotenoids, steroids, xantho proteins, couramins, alkaloids, quinones, vitamin C. The distribution of these constituents in the plant specimens were assessed and compared. The medicinal plant studied were Acalypha indica, Camellia sinensis, Plectranthus amboinicus, Curcuma longa, Rauvolfia tetraphylla. All the plant speciemens were found to contain terpenoids, xantho proteins, couramins and vitamin C. They also contain Saponins (except Curcuma longa, Combined anthroquinones (except Acalypha indica, Camellia sinensis, Curcuma longa flavonoids (except Acalypha indica, Camellia sinensis, Carotenoids (except Acalypha indica, Curcuma longa, and steroids (except Plectranthus amboinicus, Rauvolfia tetraphylla Quinones were found in one out of the five specimens. Some of the medicinal plant seemed to have potential as source of useful drugs. Though the one percent extracts of all the plants showed some degree of antimicrobial activity, it was significant in Acalypha indica, Camellia sinensis, Plectranthus amboinicus, Curcuma longa, and Rauvolfia tetraphylla. The extract of Camellia sinensis and Acalypha indica was most effective against Enterobacter faecalis (ZI = 3 cm and ZI = 1.7cm and Camellia sinensis and Acalypha indica was most effective against Staphylococcus aureus (ZI = 2.1 cm.

  6. Some Activities with Polarized Light from a Laptop LCD Screen

    Science.gov (United States)

    Fakhruddin, Hasan

    2008-01-01

    The LCD screen of a laptop computer provides a broad, bright, and extended source of polarized light. A number of demonstrations on the properties of polarized light from a laptop computer screens are presented here.

  7. Predicting Child Physical Activity and Screen Time: Parental Support for Physical Activity and General Parenting Styles

    OpenAIRE

    Langer, Shelby L; Crain, A. Lauren; Senso, Meghan M.; Levy, Rona L.; Sherwood, Nancy E

    2014-01-01

    Objective: To examine relationships between parenting styles and practices and child moderate-to-vigorous physical activity (MVPA) and screen time. Methods: Participants were children (6.9 ± 1.8 years) with a body mass index in the 70–95th percentile and their parents (421 dyads). Parent-completed questionnaires assessed parental support for child physical activity (PA), parenting styles and child screen time. Children wore accelerometers to assess MVPA. Results: Parenting style did not predi...

  8. Sleeping Beauty screen reveals Pparg activation in metastatic prostate cancer.

    Science.gov (United States)

    Ahmad, Imran; Mui, Ernest; Galbraith, Laura; Patel, Rachana; Tan, Ee Hong; Salji, Mark; Rust, Alistair G; Repiscak, Peter; Hedley, Ann; Markert, Elke; Loveridge, Carolyn; van der Weyden, Louise; Edwards, Joanne; Sansom, Owen J; Adams, David J; Leung, Hing Y

    2016-07-19

    Prostate cancer (CaP) is the most common adult male cancer in the developed world. The paucity of biomarkers to predict prostate tumor biology makes it important to identify key pathways that confer poor prognosis and guide potential targeted therapy. Using a murine forward mutagenesis screen in a Pten-null background, we identified peroxisome proliferator-activated receptor gamma (Pparg), encoding a ligand-activated transcription factor, as a promoter of metastatic CaP through activation of lipid signaling pathways, including up-regulation of lipid synthesis enzymes [fatty acid synthase (FASN), acetyl-CoA carboxylase (ACC), ATP citrate lyase (ACLY)]. Importantly, inhibition of PPARG suppressed tumor growth in vivo, with down-regulation of the lipid synthesis program. We show that elevated levels of PPARG strongly correlate with elevation of FASN in human CaP and that high levels of PPARG/FASN and PI3K/pAKT pathway activation confer a poor prognosis. These data suggest that CaP patients could be stratified in terms of PPARG/FASN and PTEN levels to identify patients with aggressive CaP who may respond favorably to PPARG/FASN inhibition.

  9. Sleeping Beauty screen reveals Pparg activation in metastatic prostate cancer.

    Science.gov (United States)

    Ahmad, Imran; Mui, Ernest; Galbraith, Laura; Patel, Rachana; Tan, Ee Hong; Salji, Mark; Rust, Alistair G; Repiscak, Peter; Hedley, Ann; Markert, Elke; Loveridge, Carolyn; van der Weyden, Louise; Edwards, Joanne; Sansom, Owen J; Adams, David J; Leung, Hing Y

    2016-07-19

    Prostate cancer (CaP) is the most common adult male cancer in the developed world. The paucity of biomarkers to predict prostate tumor biology makes it important to identify key pathways that confer poor prognosis and guide potential targeted therapy. Using a murine forward mutagenesis screen in a Pten-null background, we identified peroxisome proliferator-activated receptor gamma (Pparg), encoding a ligand-activated transcription factor, as a promoter of metastatic CaP through activation of lipid signaling pathways, including up-regulation of lipid synthesis enzymes [fatty acid synthase (FASN), acetyl-CoA carboxylase (ACC), ATP citrate lyase (ACLY)]. Importantly, inhibition of PPARG suppressed tumor growth in vivo, with down-regulation of the lipid synthesis program. We show that elevated levels of PPARG strongly correlate with elevation of FASN in human CaP and that high levels of PPARG/FASN and PI3K/pAKT pathway activation confer a poor prognosis. These data suggest that CaP patients could be stratified in terms of PPARG/FASN and PTEN levels to identify patients with aggressive CaP who may respond favorably to PPARG/FASN inhibition. PMID:27357679

  10. Screening of selected pesticides for oestrogen receptor activation in vitro

    DEFF Research Database (Denmark)

    Vinggaard, Anne; Breinholt, Vibeke; Larsen, John Christian

    1999-01-01

    Twenty pesticides were tested for their ability to activate the oestrogen receptor in vitro using an,MCF7 cell proliferation assay and a Yeast Oestrogen Screen. The fungicides fenarimol, triadimefon, and triadimenol were identified as weak oestrogen receptor agonists, which at 10 mu M induces a 2.......0, 2.4, and 1.9-fold increase in proliferation of human MCF7 breast cancer cells (E3 clone). The relative proliferation efficiency (RPE) was 43-69%, indicating partial agonism at the oestrogen receptor. Several pesticides did not have any effect oil the proliferation response after 6 days of exposure......, including. chlorpyrifos, diuron, iprodion, linuron, pentachlorphenol, prochloraz, propioconazol, propyzamine, quintozen, tetrachorvinphos and tetradifon. Some pesticides resulted in a negligible proliferation response, which was nor statistically significant under the present experimental conditions...

  11. Spectroscopic diagnostics of active screen plasma nitriding processes: on the interplay of active screen and model probe plasmas

    Science.gov (United States)

    Hamann, S.; Börner, K.; Burlacov, I.; Spies, H.-J.; Röpcke, J.

    2015-09-01

    In a reactor used for active screen plasma nitriding (ASPN) the interplay of two plasma types, (i) the plasma of the cylindrical active screen driven in a pulsed dc mode (f = 1 kHz, 60% duty cycle) and (ii) the plasma at an internal model probe driven in a cw dc mode, ignited in a low pressure H2-N2 gas mixture (p = 3 mbar) containing small amounts of CH4 and CO2 have been studied by tunable diode laser infrared absorption (TDLAS) and optical emission spectroscopy (OES) techniques. Applying in situ TDLAS the evolution of the carbon containing precursors, CH4 and CO2, and of the reaction products, NH3, HCN, CO and H2O, has been monitored. The degree of dissociation of the carbon containing precursor molecules varied between 70% and 92%. The concentrations of the reaction products were found to be in the range 1012…1015 molecules cm-3. By analyzing the development of the molecular concentrations at changes of gas mixtures and plasma power values, it was found that (i) HCN and NH3 are the main products of plasma conversion in the case of methane admixture and (ii) CO, HCN and NH3 in the carbon dioxide case. The fragmentation efficiencies of methane and carbon dioxide (RF(CH4)  ≈  1…2   ×   1015 molecules J-1, RF(CO2)  ≈  0.5…1.0   ×   1016 molecules J-1) and the respective conversion efficiencies to the product molecules (R C(product) ≈ 1013-1015 molecules J-1) have been determined for different gas mixtures and plasma power values, while the influence of probe and screen plasmas, i.e. the phenomena caused by the interplay of both plasma sources, was analyzed. The additional usage of the plasma at the model probe has a sensitive influence on the generation of the reaction products, in particular that of NH3 and HCN. With the help of OES the rotational temperature of the screen plasma could be determined, which increases with power from 770 K to 950 K. Also with power the ionic component of nitrogen molecules, i

  12. Phytochemical Screening and Aphrodisiac Activity of Asparagus racemosus

    Directory of Open Access Journals (Sweden)

    Javeed Ahmed Wani

    2011-04-01

    Full Text Available The plant Asparagus racemosus is widely distributed in the Himalayan and sub-Himalayan regions of India. Based on preliminary reports, there is a lot of interest in using the roots of this plant for treating sexual disorders. In this study, the hydro-alcoholic and aqueous extracts of the roots of Asparagus racemosus were subjected to preliminary phytochemical screening which showed the presence of saponins, carbohydrates, glycosides and mucilages. The total extracts were tested for their aphrodisiac activity in experimental rats. The hydro-alcoholic extract of Asparagus racemosus root at higher concentration (400 mg/kg body weight showed significant aphrodisiac activity on male wistar albino rats as evidenced by an increase in number of mounts and mating performance. On the other hand, hydro-alcoholic extract at lower dose (200 mg/kg. body weight and aqueous extract (400 mg/kg body weight showed moderate aphrodisiac property. Thus, in experimental rats, the results of the present study suggest that the extracts of Asparagus racemosus exert significant aphrodisiac activity. Further, detailed studies are needed to know whether in-vivo administration of the extracts is beneficial for patients suffering from sexual disorders.

  13. Overview of DOE's field screening technology development activities

    International Nuclear Information System (INIS)

    The Department of Energy (DOE) has recently created the Office of Environmental Restoration and Waste Management, into which it consolidated those activities. Within this new organization, the Office of Technology Development (OTD) is responsible for research, development, demonstration, testing, and evaluation (RDDT ampersand E) activities aimed at meeting DOE cleanup goals, while minimizing cost and risk. Site characterization using traditional drilling, sampling, and analytical methods comprises a significant part of the environmental restoration efforts in terms of both cost and time to accomplish. It can also be invasive and create additional pathways for spread of contaminants. Consequently, DOE is focusing on site characterization as one of the areas in which significant technological advances are possible which will decrease cost, reduce risk, and shorten schedules for achieving restoration goals. DOE is investing considerably in R ampersand D and demonstration activities which will improve the abilities to screen chemical, radiological, and physical parameters in the field. This paper presents an overview of the program objectives and status and reviews some of the projects which are currently underway in the area. 1 ref

  14. Bacteriophages as anti-infective agents: recent developments and regulatory challenges.

    Science.gov (United States)

    Gilmore, Brendan F

    2012-05-01

    The biennial meeting on 'Exploiting Bacteriophages for Bioscience, Biotechnology and Medicine', held in London, UK, on 20 January 2012, and chaired by George Salmond (University of Cambridge, UK) hosted over 50 participants representing 13 countries. The highly multidisciplinary meeting covered a diverse range of topics, reflecting the current expansion of interest in this field, including the use of bacteriophages as the source of biochemical reagents for molecular biology, bacteriophages for the treatment of human and animal diseases, bacteriophage-based diagnostics and therapeutic delivery technologies and necessity for, and regulatory challenges associated with, robust clinical trials of phage-based therapeutics. This report focuses on a number of presentations from the meeting relating to cutting-edge research on bacteriophages as anti-infective agents.

  15. Electrochemical screening of biomembrane-active compounds in water

    Energy Technology Data Exchange (ETDEWEB)

    Mohamadi, Shahrzad, E-mail: cmsm@leeds.ac.uk; Tate, Daniel J.; Vakurov, Alexander; Nelson, Andrew

    2014-02-01

    Graphical abstract: - Highlights: • Analytical technology application with improvement allowing for on-line high-throughput water toxin screening is presented. • Compound classes of related structure and shape interact with DOPC coated Pt/Hg with a class specific response. • Predecessor membrane system proved as fragile, complex and for environmental application incompatible. - Abstract: Interactions of biomembrane-active compounds with phospholipid monolayers on microfabricated Pt/Hg electrodes in an on-line high throughput flow system are demonstrated by recording capacitance current peak changes as rapid cyclic voltammograms (RCV). Detection limits of the compounds’ effects on the layer have been estimated from the data. Compounds studied include steroids, polycyclic aromatic hydrocarbons, tricyclic antidepressants and tricyclic phenothiazines. The results show that the extent and type of interaction depends on the—(a) presence and number of aromatic rings and substituents, (b) presence and composition of side chains and, (c) molecular shape. Interaction is only indirectly related to compound hydrophobicity. For a selection of tricyclic antidepressants and tricyclic phenothiazines the detection limit in water is related to their therapeutic normal threshold. The sensing assay has been tested in the presence of humic acid as a potential interferent and in a tap water matrix. The system can be applied to the screening of putative hazardous substances and pharmaceuticals allowing for early detection thereof in the water supply. The measurements are made in real time which means that potentially toxic compounds are detected rapidly within <10 min per assay. This technology will contribute greatly to environment safety and health.

  16. From Pichia anomala killer toxin through killer antibodies to killer peptides for a comprehensive anti-infective strategy.

    Science.gov (United States)

    Polonelli, Luciano; Magliani, Walter; Ciociola, Tecla; Giovati, Laura; Conti, Stefania

    2011-01-01

    "Antibiobodies", antibodies (Abs) with antibiotic activity, internal image of a Pichia anomala killer toxin (PaKT) characterized by microbicidal activity against microorganisms expressing β-glucans cell-wall receptors (PaKTRs), were produced by idiotypic vaccination with a PaKT-neutralizing monoclonal Ab (PaKT-like Abs) or induced by a protein-conjugated β-glucan. Human natural PaKT-like Abs (PaKTAbs) were found in the vaginal fluid of women infected with KT-sensitive microorganisms. Monoclonal and recombinant PaKT-like Abs, and PaKTAbs proved to be protective against experimental candidiasis, cryptococcosis and aspergillosis. A killer decapeptide (KP), synthesized from the sequence of a recombinant PaKT-like Ab or produced in transgenic plants, showed a microbicidal activity in vitro, neutralized by β-glucans, a therapeutic effect in vivo, against experimental mucosal and systemic mycoses, and a prophylactic role in planta, against phytopathogenic microorganisms, respectively. KP showed fungicidal properties against all the defective mutants of a Saccharomyces cerevisiae library, inclusive of strains recognized to be resistant to conventional antifungal drugs. KP inhibited in vitro, ex vivo and/or in vivo HIV-1 and Influenza A virus replication, owing to down-regulation of CCR5 co-receptors, physical block of the gp120-receptor interaction and reduction in the synthesis of glycoproteins, HA and M1 in particular. KP modulated the expression of costimulatory and MHC molecules on murine dendritic cells, improving their capacity to induce lymphocyte proliferation. KP, proven to be devoid of cytotoxicity on human cells, showed self-assembly-releasing hydrogel-like properties, catalyzed by β 1,3 glucan. PaKT's biotechnological derivatives may represent the prototypes of novel antifungal vaccines and anti-infective drugs characterized by different mechanisms of action. PMID:20714805

  17. Active screen plasma nitriding enhances cell attachment to polymer surfaces

    Energy Technology Data Exchange (ETDEWEB)

    Kaklamani, Georgia, E-mail: g.kaklamani@bham.ac.uk [University of Birmingham, College of Engineering and Physical Sciences, School of Metallurgy and Materials, Edgbaston, Birmingham B15 2TT (United Kingdom); Bowen, James; Mehrban, Nazia [University of Birmingham, College of Engineering and Physical Sciences, School of Chemical Engineering, Edgbaston, Birmingham B15 2TT (United Kingdom); Dong, Hanshan [University of Birmingham, College of Engineering and Physical Sciences, School of Metallurgy and Materials, Edgbaston, Birmingham B15 2TT (United Kingdom); Grover, Liam M. [University of Birmingham, College of Engineering and Physical Sciences, School of Chemical Engineering, Edgbaston, Birmingham B15 2TT (United Kingdom); Stamboulis, Artemis [University of Birmingham, College of Engineering and Physical Sciences, School of Metallurgy and Materials, Edgbaston, Birmingham B15 2TT (United Kingdom)

    2013-05-15

    Active screen plasma nitriding (ASPN) is a well-established technique used for the surface modification of materials, the result of which is often a product with enhanced functional performance. Here we report the modification of the chemical and mechanical properties of ultra-high molecular weight poly(ethylene) (UHMWPE) using 80:20 (v/v) N{sub 2}/H{sub 2} ASPN, followed by growth of 3T3 fibroblasts on the treated and untreated polymer surfaces. ASPN-treated UHMWPE showed extensive fibroblast attachment within 3 h of seeding, whereas fibroblasts did not successfully attach to untreated UHMWPE. Fibroblast-coated surfaces were maintained for up to 28 days, monitoring their metabolic activity and morphology throughout. The chemical properties of the ASPN-treated UHMWPE surface were studied using X-ray photoelectron spectroscopy, revealing the presence of C-N, C=N, and C≡N chemical bonds. The elastic modulus, surface topography, and adhesion properties of the ASPN-treated UHMWPE surface were studied over 28 days during sample storage under ambient conditions and during immersion in two commonly used cell culture media.

  18. Experimental techniques for screening of antiosteoporotic activity in postmenopausal osteoporosis.

    Science.gov (United States)

    Satpathy, Swaha; Patra, Arjun; Ahirwar, Bharti

    2015-12-01

    Postmenopausal osteoporosis, a silent epidemic, has become a major health hazard, afflicting about 50% of postmenopausal women worldwide and is thought to be a disease with one of the highest incidences in senile people. It is a chronic, progressive condition associated with micro-architectural deterioration of bone tissue that results in low bone mass, decreased bone strength that predisposes to an increased risk of fracture. Women are more likely to develop osteoporosis than men due to reduction in estrogen during menopause which leads to decline in bone formation and increase in bone resorption activity. Estrogen is able to suppress the production of proinflammatory cytokines like interleukin (IL)-1, IL-6, IL-7 and tumor necrosis factor (TNF-α). This is why these cytokines are elevated in postmenopausal women. In this review article we have made an attempt to collate the various methods and parameters most frequently used for screening of antiosteoporotic activity in postmenopausal osteoporosis. Pertaining to ovariectomized animal model, this is the most appropriate model for studying the efficacy of different drugs to prevent bone loss in postmenopausal osteoporosis.

  19. Screening of Azotobacter isolates for PGP properties and antifungal activity

    Directory of Open Access Journals (Sweden)

    Bjelić Dragana Đ.

    2015-01-01

    Full Text Available Аmong 50 bacterial isolates obtained from maize rhizospherе, 13 isolates belonged to the genus Azotobacter. Isolates were biochemically characterized and estimated for pH and halo tolerance ability and antibiotic resistance. According to characterization, the six representative isolates were selected and further screened in vitro for plant growth promoting properties: production of indole-3-acetic acid (IAA, siderophores, hydrogen cyanide (HCN, exopolysaccharides, phosphate solubilization and antifungal activity (vs. Helminthosporium sp., Macrophomina sp., Fusarium sp.. Beside HCN production, PGP properties were detected for all isolates except Azt7. All isolates produced IAA in the medium without L-tryptophan and the amount of produced IAA increased with concentration of precursor in medium. The highest amount of IAA was produced by isolates Azt4 (37.69 and 45.86 μg ml-1 and Azt5 (29.44 and 50.38 μg ml-1 in the medium with addition of L-tryptophan (2.5 and 5 mM. The isolates showed the highest antifungal activity against Helminthosporium sp. and the smallest antagonistic effect on Macrophomina sp. Radial Growth Inhibition (RGI obtained by the confrontation of isolates with tested phytopathogenic fungi, ranged from 10 to 48%. [Projekat Ministarstva nauke Republike Srbije, br. TR 31073

  20. Screening antimicrobial activity of various extracts of Urtica dioica.

    Science.gov (United States)

    Modarresi-Chahardehi, Amir; Ibrahim, Darah; Fariza-Sulaiman, Shaida; Mousavi, Leila

    2012-12-01

    antimicrobial activity extracts from extraction method I (33 out of 152 of crude extracts) and 6.82% from extraction method II (13 out of 190 of crude extracts). However, crude extracts from method I exhibited better antimicrobial activity against the Gram-positive bacteria than the Gram-negative bacteria. The positive results on medicinal plants screening for antibacterial activity constitutes primary information for further phytochemical and pharmacological studies. Therefore, the extracts could be suitable as antimicrobial agents in pharmaceutical and food industry. PMID:23342511

  1. Screening and antibacterial activity analysis of some important medicinal plants

    OpenAIRE

    G. Senthilmurugan Viji; B. Vasanthe; Kuru Suresh

    2013-01-01

    The screening and study of five different plant specimens belonging to different families for phytochemical constituents was performed using generally accepted laboratory technique for qualitative determinations. The constituents screened were saponins, combined anthraquinones, terpenoids, flavonoids, carotenoids, steroids, xantho proteins, couramins, alkaloids, quinones, vitamin C. The distribution of these constituents in the plant specimens were assessed and compared. The medicinal plant s...

  2. A Computational Methodology to Screen Activities of Enzyme Variants

    CERN Document Server

    Hediger, Martin R; Svendsen, Allan; Besenmatter, Werner; Jensen, Jan H

    2012-01-01

    We present a fast computational method to efficiently screen enzyme activity. In the presented method, the effect of mutations on the barrier height of an enzyme-catalysed reaction can be computed within 24 hours on roughly 10 processors. The methodology is based on the PM6 and MOZYME methods as implemented in MOPAC2009, and is tested on the first step of the amide hydrolysis reaction catalyzed by Candida Antarctica lipase B (CalB) enzyme. The barrier heights are estimated using adiabatic mapping and are shown to give barrier heights to within 3kcal/mol of B3LYP/6-31G(d)//RHF/3-21G results for a small model system. Relatively strict convergence criteria (0.5kcal/(mol{\\AA})), long NDDO cutoff distances within the MOZYME method (15{\\AA}) and single point evaluations using conventional PM6 are needed for reliable results. The generation of mutant structure and subsequent setup of the semiempirical calculations are automated so that the effect on barrier heights can be estimated for hundreds of mutants in a matte...

  3. Polyherbal preparation for anti-diabetic activity: A screening study

    Directory of Open Access Journals (Sweden)

    Noopur Srivastava

    2010-01-01

    Full Text Available Objective: To screen the Polyherbal preparation for anti-diabetic activity in rats. Materials and Methods: The blood glucose lowering activity of the Polyherbal preparation-I (1:1:1 of Wheat germ oil, Coriandrum sativum and Aloe vera was studied in normal rats after oral administration at doses of 1.0 and 2.0 ml/kg and Polyherbal preparation-I, II (Wheat germ oil, fresh juice of C. sativum and Aloe vera in the ratio of 2:2:1, and III (Wheat germ oil, fresh juice of C. sativum and Aloe vera in the ratio of 1:2:2 on alloxan-induced diabetic rats, after oral administration at doses of 1.0 and 2.0 ml/kg. Blood samples were collected from the tail vein method at 0, 0.5, 1, 2, 4, 8, 12, and 24 h in normal rats and in diabetic rats at 0, 1, 3, 7, 15, and 30 days. Blood plasma glucose was estimated by the GOD/POD (glucose oxidase and peroxidase method. The data was compared statistically using the one-way ANOVA method followed by the Dunnett multiple component test. Statistical significance was set at P<0.05. Results: The Polyherbal preparation-I produced significant (P<0.05 reduction in the blood glucose level of normal rats and Polyherbal preparation-I, II, and III produced significant (P<0.01 reduction in the blood glucose level of diabetic rats during 30 days study and compared with that of control and Glibenclamide. Conclusion: The Polyherbal preparation-I showed a significant glucose lowering effect in normal rats and Polyherbal preparation-I, II, and III in diabetic rats. This preparation is going to be promising anti-diabetic preparation for masses; however, it requires further extensive studies in human beings.

  4. Screening of anticancer activity from agarwood essential oil

    Directory of Open Access Journals (Sweden)

    Yumi Zuhanis Has-Yun Hashim

    2014-01-01

    Full Text Available Background: Agarwood is a priceless non-timber forest product from Aquilaria species belonging to the Thymelaeaceae family. As a result of a defence mechanism to fend off pathogens, Aquilaria species develop agarwood or resin which can be used for incense, perfumery, and traditional medicines. Evidences from ethnopharmacological practices showed that Aquilaria spp. have been traditionally used in the Ayurvedic practice and Chinese medicine to treat various diseases particularly the inflammatory-associated diseases. There have been no reports on traditional use of agarwood towards cancer treatment. However, this is most probably due to the fact that cancer nomenclature is used in modern medicine to describe the diseases associated with unregulated cell growth in which inflammation and body pain are involved. Objective: The aim of this current study was therefore to investigate the potential anticancer properties of agarwood essential oil obtained from distillation of agarwood (resin towards MCF-7 breast cancer cells. Materials and Methods: The essential oil was subjected to screening assays namely cell viability, cell attachment and sulforhodamine B (SRB-based cytotoxicity assay to determine the IC 50 value. Results: The agarwood essential oil caused reduction of the cell number in both the cell viability and attachment assay suggesting a cumulative effect of the cell killing, inhibition of the cell attachment and or causing cells to detach. The agarwood essential oil showed IC 50 value of 900 μg/ml towards the cancer cells. Conclusion: The agarwood essential oil exhibited anticancer activity which supports the traditional use against the inflammatory-associated diseases. This warrants further investigation towards the development of alternative remedy towards cancer.

  5. Electrodermal screening of biologically active points for upper gastrointestinal bleeding.

    Science.gov (United States)

    Tseng, Ying-Jung; Hu, Wen-Long; Hung, I-Ling; Hsieh, Chia-Jung; Hung, Yu-Chiang

    2014-01-01

    The purpose of this case-control study was to investigate the relationship between the electrical resistance of the skin at biologically active points (BAPs) on the main meridians and upper gastrointestinal bleeding (UGIB). Electrical resistance to direct current at 20 BAPs on the fingers and toes of 100 patients with (38 men, 12 women; mean age [range], 58.20 ± 19.62 [18-83] years) and without (27 men, 23 women; 49.54 ± 12.12 [22-74] years) UGIB was measured through electrodermal screening (EDS), based on the theory of electroacupuncture according to Voll (EAV). Data were compared through analysis of variance (ANOVA), receiver operating characteristic (ROC) curve analysis, and logistic regression. The initial readings were lower in the UGIB group, indicating blood and energy deficiency due to UGIB. Significant differences in indicator drop values were observed at nine BAPs (p < 0.05) on the bilateral small intestine, bilateral stomach, bilateral circulation, bilateral fibroid degeneration, and right lymph meridians. The area under the ROC curve values of the BAPs on the bilateral small intestine and stomach meridians were larger than 0.5, suggesting the diagnostic accuracy of EDS for UGIB on the basis of the indicator drop of these BAPs. Logistic regression revealed that when the indicator drop of the BAP on the left stomach meridian increased by one score, the risk of UGIB increased by about 1.545-3.523 times. In conclusion, the change in the electrical resistance of the skin measured by EDS at the BAPs on the bilateral small intestine and stomach meridians provides specific information on UGIB.

  6. Phytochemical Screening and Pharmacological Activities of Entada Scandens seeds

    Directory of Open Access Journals (Sweden)

    S K Dey

    2013-03-01

    can form an excellent source for derivation of lead compounds or newer drugs. The knowledge base of folk medicinal practitioners can in this instance form an invaluable source on which further scientific studies may be based, for the folk medicinal practices of the Kavirajes date back to centuries ago. They also have proved to be a rich source of new active compounds which are less toxic and less costly when compared to the synthetic drugs. The present study will help the industry to produce herbal drug with less side effect, economically affordable and more effective in the treatment of pain, diarrhea and inflammation processes. Finally the phytochemical screening from the plant would be effective drug for the antinociceptive, cytotoxic and antidiarrheal activities of the crude ethanol extract of the seed of E. scandens. Keywords: Entada scandens; Phytochemical; Antinociceptive; Anti-diarrheal; Cytotoxic.

  7. Health complaints among adolescents: Associations with more screen-based behaviours and less physical activity.

    Science.gov (United States)

    Marques, Adilson; Calmeiro, Luís; Loureiro, Nuno; Frasquilho, Diana; de Matos, Margarida Gaspar

    2015-10-01

    In this study, we investigated the relationship between screen-based behaviours, physical activity, and health complaints (headaches, feeling low, irritability, and nervousness). Screen-based behaviour included TV viewing, computer use, and time spent playing video games. Data were collected from 4462 Portuguese adolescents (2394 girls) aged 11-16 years. Girls who reported engaging in more screen-based behaviour (hours/day) also reported having more headaches, feeling lower, being more irritable, and feeling more nervous. Boys who reported more screen time were more irritable. Physical activity (times/week) was negatively associated with reports of feeling nervous among girls, and with headaches, feeling low, irritability, and feeling nervous among boys. Considering that time spent using the computer is related with more health complaints, and physical activity was related with fewer health complaints among boys, it is important to develop strategies to reduce adolescents' computer screen time, and to promote physical activity. PMID:26275746

  8. Destination state screening of active spaces in spin dynamics simulations

    Science.gov (United States)

    Krzystyniak, M.; Edwards, Luke J.; Kuprov, Ilya

    2011-06-01

    We propose a novel avenue for state space reduction in time domain Liouville space spin dynamics simulations, using detectability as a selection criterion - only those states that evolve into or affect other detectable states are kept in the simulation. This basis reduction procedure (referred to as destination state screening) is formally exact and can be applied on top of the existing state space restriction techniques. As demonstrated below, in many cases this results in further reduction of matrix dimension, leading to considerable acceleration of many spin dynamics simulation types. Destination state screening is implemented in the latest version of the Spinach library (http://spindynamics.org).

  9. Anti-infection activity of nanostructured titanium percutaneous implants with a postoperative infection model

    International Nuclear Information System (INIS)

    Highlights: • We prepared three titania nanotubes (TNT-50, TNT-100, TNT-150) on titanium surfaces by anodization. • TNT-100 had the highest antibacterial efficiency under the visible light. • The immersion test in the culture medium suggested that TNT can adsorb more proteins than pTi. • TNT implants inhibited the infection risk and enhanced tissue integration of the percutaneous implants compared to pTi. - Abstract: The titanium percutaneous implants were widely used in clinic; however, they have an increased risk of infection since they breach the skin barrier. Lack of complete skin integration with the implants can cause infection and implant removal. In this work, three titania nanotubes (TNT) with different diameters, 50 nm (TNT-50), 100 nm (TNT-100) and 150 nm (TNT-150) arrays were prepared on titanium surfaces by anodization, pure titanium (pTi) was used as control. Samples were characterized by scanning electron microscopy (SEM), atomic force microscopy (AFM), and contact angle analysis. The antibacterial efficiency of TNT was evaluated in vitro against Staphylococcus aureus under the visible light. The results indicated that TNT-100 had the highest antibacterial efficiency under the visible light. Subsequently, TNT implants and pTi implants were placed subcutaneously to the dorsum of New Zealand White rabbits, 108 CFU S. aureus was inoculated into the implant sites 4 h after surgery. The TNF-alpha and IL-1alpha were determined using enzyme linked immunoassay (ELISA). TNT implants revealed less inflammatory factor release than pTi implants with or without injected S. aureus liquid. According to the histological results, the TNT implants displayed excellent tissue integration. Whereas, pTi implants were surrounded with fibrotic capsule, and the skin tissue was almost separated from the implant surface. Therefore, the TNT significantly inhibited the infection risk and enhanced tissue integration of the percutaneous implants compared to pTi. The immersion test in the culture medium suggested that one of causes be probably more proteins adsorbed on TNT than on pTi

  10. Anti-infection activity of nanostructured titanium percutaneous implants with a postoperative infection model

    Energy Technology Data Exchange (ETDEWEB)

    Tan, Jing; Li, Yiting; Liu, Zhiyuan; Qu, Shuxin; Lu, Xiong; Wang, Jianxin; Duan, Ke; Weng, Jie; Feng, Bo, E-mail: fengbo@swjtu.edu.cn

    2015-07-30

    Highlights: • We prepared three titania nanotubes (TNT-50, TNT-100, TNT-150) on titanium surfaces by anodization. • TNT-100 had the highest antibacterial efficiency under the visible light. • The immersion test in the culture medium suggested that TNT can adsorb more proteins than pTi. • TNT implants inhibited the infection risk and enhanced tissue integration of the percutaneous implants compared to pTi. - Abstract: The titanium percutaneous implants were widely used in clinic; however, they have an increased risk of infection since they breach the skin barrier. Lack of complete skin integration with the implants can cause infection and implant removal. In this work, three titania nanotubes (TNT) with different diameters, 50 nm (TNT-50), 100 nm (TNT-100) and 150 nm (TNT-150) arrays were prepared on titanium surfaces by anodization, pure titanium (pTi) was used as control. Samples were characterized by scanning electron microscopy (SEM), atomic force microscopy (AFM), and contact angle analysis. The antibacterial efficiency of TNT was evaluated in vitro against Staphylococcus aureus under the visible light. The results indicated that TNT-100 had the highest antibacterial efficiency under the visible light. Subsequently, TNT implants and pTi implants were placed subcutaneously to the dorsum of New Zealand White rabbits, 10{sup 8} CFU S. aureus was inoculated into the implant sites 4 h after surgery. The TNF-alpha and IL-1alpha were determined using enzyme linked immunoassay (ELISA). TNT implants revealed less inflammatory factor release than pTi implants with or without injected S. aureus liquid. According to the histological results, the TNT implants displayed excellent tissue integration. Whereas, pTi implants were surrounded with fibrotic capsule, and the skin tissue was almost separated from the implant surface. Therefore, the TNT significantly inhibited the infection risk and enhanced tissue integration of the percutaneous implants compared to pTi. The immersion test in the culture medium suggested that one of causes be probably more proteins adsorbed on TNT than on pTi.

  11. A comparison of protein kinases inhibitor screening methods using both enzymatic activity and binding affinity determination

    DEFF Research Database (Denmark)

    Rudolf, Amalie Frederikke; Skovgaard, Tine; Knapp, Stefan;

    2014-01-01

    Binding assays are increasingly used as a screening method for protein kinase inhibitors; however, as yet only a weak correlation with enzymatic activity-based assays has been demonstrated. We show that the correlation between the two types of assays can be improved using more precise screening...

  12. In silico screening of 393 mutants facilitates enzyme engineering of amidase activity in CalB

    DEFF Research Database (Denmark)

    Hediger, Martin Robert; De Vico, Luca; Rannes, Julie Bille;

    2013-01-01

    Our previously presented method for high throughput computational screening of mutant activity (Hediger et al., 2012) is benchmarked against experimentally measured amidase activity for 22 mutants of Candida antarctica lipase B (CalB). Using an appropriate cutoff criterion for the computed barriers......, the qualitative activity of 15 out of 22 mutants is correctly predicted. The method identifies four of the six most active mutants with ≥3-fold wild type activity and seven out of the eight least active mutants with ≤0.5-fold wild type activity. The method is further used to screen all sterically possible (386...

  13. Estimation of the front-to-total activity ratio for wire screens using CFD simulation.

    Science.gov (United States)

    Chen, B; Zhuo, W

    2015-11-01

    Wire screens are widely used for sampling radioactive aerosols. The front-to-total activity ratio is a critical factor in describing the self-shielding effect of the wire screens. In this study, computational fluid dynamic method was applied to simulate the deposition of aerosols on the surface of the wire screens. Four different types of screens were investigated for particle size varying from 1 nm to 10 µm. Experimental verification was carried out in a radon chamber. The results showed good agreement between experimental data interception and the simulation. Significant differences on the front-to-total activity ratio for the different types of screens were observed when the size of particle was <20 nm. PMID:25920787

  14. 75 FR 9915 - Extension of Agency Information Collection Activity Under OMB Review: Certified Cargo Screening...

    Science.gov (United States)

    2010-03-04

    ...-airport and includes facilties upstream in the air cargo supply chain, such as shippers, manufacturers... SECURITY Transportation Security Administration Extension of Agency Information Collection Activity Under OMB Review: Certified Cargo Screening Program AGENCY: Transportation Security Administration,...

  15. 76 FR 4709 - Extension of Agency Information Collection Activity Under OMB Review: Certified Cargo Screening...

    Science.gov (United States)

    2011-01-26

    ... off- airport and includes facilities upstream in the air cargo supply chain, such as shippers... supply chain to accept, screen, and transport air cargo. The uninterrupted collection of this information... SECURITY Transportation Security Administration Extension of Agency Information Collection Activity...

  16. 77 FR 25187 - Extension of Agency Information Collection Activity Under OMB Review: Certified Cargo Screening...

    Science.gov (United States)

    2012-04-27

    ... and include facilties upstream ] in the air cargo supply chain, such as shippers, manufacturers... SECURITY Transportation Security Administration Extension of Agency Information Collection Activity Under OMB Review: Certified Cargo Screening Program AGENCY: Transportation Security Administration,...

  17. Screening of some traditionally used medicinal plants for potential antibacterial activity

    OpenAIRE

    Parekh Jigna; Karathia Nehal; Chanda Sumitra

    2006-01-01

    In the present work an attempt has been made to carry out screening for the preliminary antibacterial activity of different plants used in Indian folk medicine. The aim of the study was to select an active plant extract which may be useful in developing new lead compounds to combat deadly diseases. Twelve plants were selected for preliminary screening for their antibacterial potentiality, viz., Abutilon indicum L., Acorous calamus L., Ammania baccifera L., Argyrea nervosa Burm. F., B...

  18. A comparison of hamstring muscle activity during different screening tests for non-contact ACL injury

    DEFF Research Database (Denmark)

    Husted, Rasmus S.; Bencke, Jesper; Andersen, Lars L.;

    2016-01-01

    phenomenon and thereby observable independently of the type of clinical screening tests used is not known. This cross sectional study investigated the rank correlation of knee joint neuromuscular activity between three different ACL injury risk screening tests. METHODS: Sixty-two adolescent female elite......-activity, correlation analysis (Spearman correlation coefficient) showed low-to-moderate correlations between SC and 1) DJ (rs=0.34-0.36, P

  19. Autecology Essential Oil Composition, Antibacterial, Anti Candidacies and Ethnopharmacological Survey of Ferula Gummosa L. As Anti Infection to Treat Of Vaginal Infections in Traditional Medicine of Razavi Khorasan Province (North East of Iran

    Directory of Open Access Journals (Sweden)

    Mazandarani Masoumeh

    2015-04-01

    Full Text Available Objective: Ferula gummosa Boiss. (Apiaceae family, which has been used in traditional medicine of Iran as anti vaginal infection, anti-sinusitis, sedative, and anti-inflammation. Materials and Methods: In this research, the gums of plant root were collected from the Heidary nature reserve in Razavi Khorasan Province (Iran in August 2012. The ethnopharmacological data about traditional uses of plant were obtained from the rural healers (women 67-75 year of this region. Essential oil of the plant root gum was obtained by hydrodistillation (Clevenger apparatus and was analyzed by gas chromatography–mass spectrometry. Antibacterial activity of plant ethanolic extract was studied in vitro against Candida albicans and 9 Gram-positive and negative bacteria using well method and the minimum inhibitory concentration (MIC assay. Results: Results showed that a total of 39 components have been identified in the plant sampl oil, representing 81% of the total oil and β-pinene (19.88%, guaiol (8%, shyobunone (6.96%, delta-cadinene (4.65%, α-pinene (3.16 %, β-phellandrene (3.28% and myrtenol (2.8%, were the main essential oil composition, respectively. The results from antibacterial screening (Table 2, were showed that C. albicans (25.2 ± 1.6, Staphylococcus epidermidis (23.6 ± 0.7 mm, Staphylococcus aureus (21.3 ± 0.2 mm, Escherichia coli (16.5 ± 0.8 mm, Bacillus cereus (19.5 ± 0.1 mm, Enterococcus faecalis (17.2 ± 0.8 mm and Pseudomonas aeroginosa ( 17.8 ± 0.2 mm inhibition zone and MIC (35.4-112 μg/ml were the most sensitive pathogenes to the plant extract respectively, which followed Shigella (12.3 ± 0.3 mm and Klebsiella pneumonia (12.5 ± 0.2 mm were found to be moderate sensitive bacteria and then the Salmonella typhymorium which completely was resistant to plant root extract. Conclusion: According to these results, it can be concluded that the extract of F. gummosa L. have suitable antimicrobial and anti-Candidacies activity, which can be

  20. Virtual Screening Analysis and In-vitro Xanthine Oxidase Inhibitory Activity of Some Commercially Available Flavonoids

    OpenAIRE

    Umamaheswari, Muthuswamy; Madeswaran, Arumugam; Asokkumar, Kuppusamy

    2013-01-01

    Allopurinol, the xanthine oxidase inhibitor, is the only drug available for the treatment of gout. We examined the xanthine oxidase inhibitory activity of some commercially available flavonoids such asepigallocatechin, acacatechin, myricetin, naringenin, daidzein and glycitein by virtual screening and in-vitro studies. The interacting residues within the complex model and their contact types were identified. The virtual screening analysis were carried out using AutoDock 4.2 and in-vitro xanth...

  1. Screening assays for primary haemophagocytic lymphohistiocytosis in children presenting with suspected macrophage activation syndrome

    OpenAIRE

    Cruikshank, M; Anoop, P; Nikolajeva, O.; Rao, A; Rao, K.; Gilmour, K.; Eleftheriou, D; Brogan, P. A.

    2014-01-01

    Background Primary haemophagocytic lymphohistiocytosis (HLH) screening assays are increasingly being performed in patients presenting with macrophage activation syndrome (MAS). The objective of this study was to describe their diagnostic and prognostic relevance in children who had presented to paediatric rheumatology and had undergone investigative work up for MAS. Methods Data was obtained retrospectively from an existing protein screening assay database and patient records. Assays included...

  2. Screening of some Malay medicated oils for antimicrobial activity

    Directory of Open Access Journals (Sweden)

    Khalid Khalisanni

    2010-01-01

    Full Text Available Oils from six Malay medicated oils, used traditionally in the treatment of infectious and septic diseases in humans, were tested for their antimicrobial property. The aim was to evaluate the antimicrobial properties of six Malay medicated oils against certain microbial isolates. Locally available Malay medicated oils were checked for their antimicrobial activities using six species of bacteria: E. coli, Salmonella spp., Klebsiella pneumoniae, Staphylococcus aureus, Streptococcus, Bacillus subtilis and 2 fungi with 1 yeast (Aspergillus niger, Penicillum spp. and Candida albicans. Clove oil showed the highest antibacterial activity followed, respectively, by 'bunga merah', cajaput, nutmeg, lemon grass and 'gamat' oil. Clove oil and lemon grass showed anticandidal activity. The Malay medicated oil studies did not show any antifungal activity. The study shows that Malay medicated oils, like antibiotics, have antimicrobial activities against some microorganisms.

  3. Engineering Chiral Catalysts through Asymmetric Activation and Super High Throughput Screening (SHTS)

    Institute of Scientific and Technical Information of China (English)

    MIKAMI,Koichi; KORENAGA,Toshinobu; MATSUKAWA,Satoru; DING,Kui-Ling; LONG,Jiang

    2001-01-01

    A conceptually new strategy for asymmetric catalysis, namely asymmetric activation, in which a chiral activator selectively activates one enantiomer of a racemic chiral catalyst, and a highly efficient screening system for finding the most effective catalysts, namely super high throughput screening (SHTS), by which the reaction can be conducted in parallel and the ee% of the product is allowed to determine within minutes, are summarized in the present account. It is reasonable to be lieve that SHTS technique combined with asymmetric activa tion or deactivation principle will provide a very powerful methodology for finding the new catalysts and the best catalyst tuning for asymmetric reactions.

  4. ANTIOXIDANT ACTIVITY AND PHARMACOLOGICAL SCREENING OF TINOSPORA CORDIFOLIA (THUNB.)

    OpenAIRE

    M. P. SINHA; SUKUMAR DANDAPAT; MANOJ KUMAR; AMIT KUMAR

    2013-01-01

    The communication deals with the antioxidant activity of aqueous and methanolic extracts of Tinospora cordifolia(Thunb.) stem, along with the phytochemical, pharmacological and nutritive properties. Methanolic extractshowed good antioxidant efficacy compare to the BHA standard. Reducing power of the extract showedconcentration dependence. Lipid peroxidation inhibition was not significant. Methanolic extract showed significantDPPH radical scavenging activity (EC50 = 0.5 mg/mL), while the super...

  5. A Potent Activator of Melanogenesis Identified from Small Molecule Screening

    OpenAIRE

    McNaughton, Brian R.; Gareiss, Peter C.; Jacobs, Stacey E.; Fricke, Alex F.; Scott, Glynis A.; Miller, Benjamin L.

    2009-01-01

    Small molecules that increase the cellular level of melanin can be used to study melanogenesis, and have therapeutic potential for melanin-related diseases such as albinism. We describe the identification of a potent activator of melanogenesis from a targeted combinatorial library. Treating melanocytes with our most active molecule results in a 1.8-fold increase in melanin, and an increase in tyrosinase-catalyzed oxidation of L-tyrosine, a key step in melanin biosynthesis.

  6. Screening of flocculant-producing microorganisms and flocculating activity

    Institute of Scientific and Technical Information of China (English)

    CHENG Jin-ping; ZHANG Lan-ying; WANG Wen-hua; YANG Yi-chen; ZHENG Min; JU Su-wei

    2004-01-01

    A strain saccharomycete STSM-1 with high flocculanting activity was isolated from activated sludge with conventional methods. The high production rate and the low cost STSM-1 medium was obtained by selecting different kinds of media, carbon source, nitrogen source and inorganic salt ion. The best flocculant- producing conditions were found by changing medium initial pH, culture temperature and ventilation flow. The best flocculating effect was obtained by changing positive ion types, density and concentration of flocculant.

  7. Antitubercular activity and phytochemical screening of selected medicinal plants

    Directory of Open Access Journals (Sweden)

    Rajandeep Kaur

    2015-03-01

    Full Text Available Medicinal plants offer a hope for developing alternate medicines for the treatment of Tuberculosis.. The present study was done to evaluate in vitro anti-tubercular activity of five medicinal plants viz., Syzygium aromaticum, Piper nigrum, Glycyrrhiza glabra, Aegele marmelos and Lawsonia inermis. Solvent extracts of Syzygium aromaticum, Piper nigrum, Glycyrrhiza glabra, Aegele marmelos and Lawsonia inermis were tested in vitro for their activity against Mycobacterium tuberculosis H37Rv strain using Microplate Alamar Blue Assay. Activity in MABA was evaluated by lowest concentration of sample that prevents color change to pink. Extracts of all the five plants Syzygium aromaticum, Piper nigrum, Glycyrrhiza glabra, Aegele marmelos and Lawsonia inermis exhibited anti-tuberculosis activity, the proportion of inhibition of these plants extracts for M. tuberculosis H37Rv, inhibition was found to be 0.8µg/ml, 50µg/ml, 12.5µg/ml and 50µg/ml respectively. Our findings showed that all these plants exhibited activity against MDR isolates of H37Rv M. tuberculosis strain. Further studies aimed at isolation and identification of active substances from the extracts needs to be carried out

  8. New approach for high-throughput screening of drug activity on Plasmodium liver stages.

    NARCIS (Netherlands)

    Gego, A.; Silvie, O.; Franetich, J.F.; Farhati, K.; Hannoun, L.; Luty, A.J.F.; Sauerwein, R.W.; Boucheix, C.; Rubinstein, E.; Mazier, D.

    2006-01-01

    Plasmodium liver stages represent potential targets for antimalarial prophylactic drugs. Nevertheless, there is a lack of molecules active on these stages. We have now developed a new approach for the high-throughput screening of drug activity on Plasmodium liver stages in vitro, based on an infrare

  9. A modified reverse one-hybrid screen identifies transcriptional activation in Phyochrome-Interacting Factor 3

    Science.gov (United States)

    Transcriptional activation domains (TAD) are difficult to predict and identify, since they are not conserved and have little consensus. Here, we describe a yeast-based screening method that is able to identify individual amino acid residues involved in transcriptional activation in a high throughput...

  10. ANTIMICROBIAL ACTIVITY AND PHOTOCHEMICAL SCREENING OF TINOSPORA CORDIFOLIA AND EUPHORBIA HIRTA

    OpenAIRE

    Amit Sandhu; Neha bhardwaj; Vikas Menon; Ruby Gupta

    2013-01-01

    The present study deals with the antimicrobial activity and phytochemical screening of the two medicinal plants, Tinospora cordifolia and Euphorbia hirta those are commonly available in India. Results of antimicrobial activity revealed that these medicinal plant extracts were very effective against Serratia marcescens, E. coli, Streptococcus thermophilus, Fusarium oxysporium, Aspergillus niger while these extracts showed very less inhibition against Trichoderma reesei. Phytochemical analysis ...

  11. Silver Nanoparticles/Ibuprofen-Loaded Poly(l-lactide Fibrous Membrane: Anti-Infection and Anti-Adhesion Effects

    Directory of Open Access Journals (Sweden)

    Shuai Chen

    2014-08-01

    Full Text Available Infection caused by bacteria is one of the crucial risk factors for tendon adhesion formation. Silver nanoparticles (AgNP-loaded physical barriers were reported to be effective in anti-infection and anti-adhesion. However, high silver load may lead to kidney and liver damages. This study was designed for Ibuprofen (IBU-loaded poly(l-lactide (PLLA electrospun fibrous membranes containing a low dosage of Ag to evaluate its potential in maintaining suitable anti-infection and good anti-adhesion effects. The in vitro drug release study showed a sustained release of Ag ions and IBU from the membrane. Inferior adherence and proliferation of fibroblasts were found on the Ag4%–IBU4%-loaded PLLA electrospun fibrous membranes in comparison with pure PLLA and 4% Ag-loaded PLLA membranes. In the antibacterial test, all Ag-loaded PLLA electrospun fibrous membranes prevented the adhesion of Staphylococcus aureus and Staphylococcus epidermidis. Taken together, these results demonstrate that Ibuprofen is effective in enhancing the anti-adhesion and anti-proliferation effects of 4% Ag-loaded PLLA fibrous membrane. The medical potential of infection reduction and adhesion prevention of Ag4%–IBU4%-loaded PLLA electrospun fibrous membrane deserves to be further studied.

  12. An Active Learning Classifier for Further Reducing Diabetic Retinopathy Screening System Cost

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    Yinan Zhang

    2016-01-01

    Full Text Available Diabetic retinopathy (DR screening system raises a financial problem. For further reducing DR screening cost, an active learning classifier is proposed in this paper. Our approach identifies retinal images based on features extracted by anatomical part recognition and lesion detection algorithms. Kernel extreme learning machine (KELM is a rapid classifier for solving classification problems in high dimensional space. Both active learning and ensemble technique elevate performance of KELM when using small training dataset. The committee only proposes necessary manual work to doctor for saving cost. On the publicly available Messidor database, our classifier is trained with 20%–35% of labeled retinal images and comparative classifiers are trained with 80% of labeled retinal images. Results show that our classifier can achieve better classification accuracy than Classification and Regression Tree, radial basis function SVM, Multilayer Perceptron SVM, Linear SVM, and K Nearest Neighbor. Empirical experiments suggest that our active learning classifier is efficient for further reducing DR screening cost.

  13. An Active Learning Classifier for Further Reducing Diabetic Retinopathy Screening System Cost

    Science.gov (United States)

    An, Mingqiang

    2016-01-01

    Diabetic retinopathy (DR) screening system raises a financial problem. For further reducing DR screening cost, an active learning classifier is proposed in this paper. Our approach identifies retinal images based on features extracted by anatomical part recognition and lesion detection algorithms. Kernel extreme learning machine (KELM) is a rapid classifier for solving classification problems in high dimensional space. Both active learning and ensemble technique elevate performance of KELM when using small training dataset. The committee only proposes necessary manual work to doctor for saving cost. On the publicly available Messidor database, our classifier is trained with 20%–35% of labeled retinal images and comparative classifiers are trained with 80% of labeled retinal images. Results show that our classifier can achieve better classification accuracy than Classification and Regression Tree, radial basis function SVM, Multilayer Perceptron SVM, Linear SVM, and K Nearest Neighbor. Empirical experiments suggest that our active learning classifier is efficient for further reducing DR screening cost.

  14. Screening for Antiviral Activities of Isolated Compounds from Essential Oils

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    Akram Astani

    2011-01-01

    Full Text Available Essential oil of star anise as well as phenylpropanoids and sesquiterpenes, for example, trans-anethole, eugenol, β-eudesmol, farnesol, β-caryophyllene and β-caryophyllene oxide, which are present in many essential oils, were examined for their antiviral activity against herpes simplex virus type 1 (HSV-1 in vitro. Antiviral activity was analyzed by plaque reduction assays and mode of antiviral action was determined by addition of the drugs to uninfected cells, to the virus prior to infection or to herpesvirus-infected cells. Star anise oil reduced viral infectivity by >99%, phenylpropanoids inhibited HSV infectivity by about 60–80% and sesquiterpenes suppressed herpes virus infection by 40–98%. Both, star anise essential oil and all isolated compounds exhibited anti-HSV-1 activity by direct inactivation of free virus particles in viral suspension assays. All tested drugs interacted in a dose-dependent manner with herpesvirus particles, thereby inactivating viral infectivity. Star anise oil, rich in trans-anethole, revealed a high selectivity index of 160 against HSV, whereas among the isolated compounds only β-caryophyllene displayed a high selectivity index of 140. The presence of β-caryophyllene in many essential oils might contribute strongly to their antiviral ability. These results indicate that phenylpropanoids and sesquiterpenes present in essential oils contribute to their antiviral activity against HSV.

  15. Screening of Australian plants for antimicrobial activity against Campylobacter jejuni.

    Science.gov (United States)

    Kurekci, Cemil; Bishop-Hurley, Sharon L; Vercoe, Philip E; Durmic, Zoey; Al Jassim, Rafat A M; McSweeney, Christopher S

    2012-02-01

    Campylobacter jejuni is the most common cause of acute enteritis in humans, with symptoms such as diarrhoea, fever and abdominal cramps. In this study, 115 extracts from 109 Australian plant species were investigated for their antimicrobial activities against two C. jejuni strains using an in vitro broth microdilution assay. Among the plants tested, 107 (93%) extracts showed activity at a concentration between 32 and 1024 µg/mL against at least one C. jejuni strain. Seventeen plant extracts were selected for further testing against another six C. jejuni strains, as well as Campylobacter coli, Escherichia coli, Salmonella typhimurium, Bacillus cereus, Proteus mirabilis and Enterococcus faecalis. The extract from Eucalyptus occidentalis demonstrated the highest antimicrobial activity, with an inhibitory concentration of 32 µg/mL against C. jejuni and B. cereus. This study has shown that extracts of selected Australian plants possess antimicrobial activity against C. jejuni and thus may have application in the control of this organism in live poultry and retail poultry products.

  16. Screening of selected Indian medicinal plants for acetylcholinesterase inhibitory activity.

    Science.gov (United States)

    Vinutha, B; Prashanth, D; Salma, K; Sreeja, S L; Pratiti, D; Padmaja, R; Radhika, S; Amit, A; Venkateshwarlu, K; Deepak, M

    2007-01-19

    Seventy-six plant extracts including methanolic and successive water extracts from 37 Indian medicinal plants were investigated for acetylcholinesterase (AChE) inhibitory activity (in vitro). Results indicated that methanolic extracts to be more active than water extracts. The potent AChE inhibiting methanolic plant extracts included Withania somnifera (root), Semecarpus anacardium (stem bark), Embelia ribes (Root), Tinospora cordifolia (stem), Ficus religiosa (stem bark) and Nardostachys jatamansi (rhizome). The IC(50) values obtained for these extracts were 33.38, 16.74, 23.04, 38.36, 73.69 and 47.21mug/ml, respectively. These results partly substantiate the traditional use of these herbs for improvement of cognition. PMID:16950584

  17. Cytotoxic activity screening of Bangladeshi medicinal plant extracts.

    Science.gov (United States)

    Akter, Raushanara; Uddin, Shaikh J; Grice, I Darren; Tiralongo, Evelin

    2014-01-01

    The cytotoxic activity of 23 crude methanol extracts from 19 Bangladeshi medicinal plants was investigated against healthy mouse fibroblasts (NIH3T3), healthy monkey kidney (VERO) and four human cancer cell lines (gastric, AGS; colon, HT-29; and breast, MCF-7 and MDA-MB-231) using MTT assay. High cytotoxicity across all cell lines tested was exhibited by Aegiceras corniculatum (fruit) and Hymenodictyon excelsum (bark) extracts (IC50 values ranging from 0.0005 to 0.9980 and 0.08 to 0.44 mg/mL, respectively). Fourteen extracts from 11 plant species, namely Clitoria ternatea (flower and leaf), Dillenia indica (leaf), Diospyros peregrina (leaf), Dipterocarpus turbinatus (bark and leaf), Ecbolium viride (leaf), Glinus oppositifolius (whole plant), Gnaphalium luteoalbum (leaf), Jasminum sambac (leaf), Lannea coromandelica (bark and leaf), Mussaenda glabrata (leaf) and Saraca asoca (leaf), were also significantly cytotoxic (IC50 ternatea (flower and leaf), Caesalpinia pulcherrima (leaf), E. viride (leaf) and G. oppositifolius (whole plant) showed cytotoxicity only against both of the breast cancer cell lines (MCF-7 and MDA-MB-231). In contrast, C. ternatea (flower and leaf) exhibited high cytotoxic activity against MDA-MB-231 (IC50 values of 0.11 and 0.49 mg/mL, respectively), whereas E. viride and G. oppositifolius whole plant extracts exhibited high activity against MCF-7 cells (IC50 values of 0.06 and 0.15 mg/mL, respectively). The cytotoxic activity test results for 9 of the plant species correlate with their traditional use as anticancer agents, thus making them interesting sources for further drug development. PMID:23846168

  18. ANTIOXIDANT ACTIVITY AND PHARMACOLOGICAL SCREENING OF TINOSPORA CORDIFOLIA (THUNB.

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    M. P. SINHA

    2013-01-01

    Full Text Available The communication deals with the antioxidant activity of aqueous and methanolic extracts of Tinospora cordifolia(Thunb. stem, along with the phytochemical, pharmacological and nutritive properties. Methanolic extractshowed good antioxidant efficacy compare to the BHA standard. Reducing power of the extract showedconcentration dependence. Lipid peroxidation inhibition was not significant. Methanolic extract showed significantDPPH radical scavenging activity (EC50 = 0.5 mg/mL, while the superoxide radical scavenging activity of themethanolic extract was mild and showed concentration dependence. The phytochemical analysis showed lowamount of total ash content, i.e. 11.3 ± 1.4 mg/g. Total phenol, tannin and flavonoids contents were 17.3 ± 0.4,13.8 ± 0.5 and 6.5 ± 0.2 mg/g respectively which fall under moderate range. Crude fiber and moisture contents(231 ± 3.2 and 214 ± 5.3 mg/g respectively as well as carbohydrate content (184.1 ± 5.2 mg/g and nutritivevalue (1.46 ± 0.3 cal/g were significantly high. T. cordifolia stem showed high swelling and foaming indices,400 ± 3.5% and 111.12 ± 2.1% respectively, which is an indication of good drug release characteristics.Present findings suggest Tinospora cordifolia as potential source of natural antioxidant, fiber and nutrient contentin food, fodder and pharmaceutical industries.

  19. Screening chemicals for thyroid-disrupting activity: A critical comparison of mammalian and amphibian models.

    Science.gov (United States)

    Pickford, Daniel B

    2010-11-01

    In order to minimize risks to human and environmental health, chemical safety assessment programs are being reinforced with toxicity tests more specifically designed for detecting endocrine disrupters. This includes the necessity to detect thyroid-disrupting chemicals, which may operate through a variety of modes of action, and have potential to impair neurological development in humans, with resulting deficits of individual and social potential. Mindful of these concerns, the consensus favors in vivo models for both hazard characterization (testing) and hazard identification (screening) steps, in order to minimize false negatives. Owing to its obligate dependence on thyroid hormones, it has been proposed that amphibian metamorphosis be used as a generalized vertebrate model for thyroid function in screening batteries for detection of thyroid disrupters. However, it seems unlikely that such an assay would ever fully replace in vivo mammalian assays currently being validated for human health risk assessment: in its current form the amphibian metamorphosis screening assay would not provide capacity for reliably detecting other modes of endocrine-disrupting activity. Conversely, several candidate mammalian screening assays appear to offer robust capacity to detect a variety of modes of endocrine-disrupting activity, including thyroid activity. To assess whether omission of an amphibian metamorphosis assay from an in vivo screening battery would generate false negatives, the response of amphibian and mammalian assays to a variety known thyroid disrupters, as reported in peer-reviewed literature or government agency reports, was critically reviewed. Of the chemicals investigated from the literature selected (41), more had been tested in mammalian studies with thyroid-relevant endpoints (32) than in amphibian assays with appropriate windows of exposure and developmental endpoints (27). One chemical (methoxychlor) was reported to exhibit thyroid activity in an appropriate

  20. Extracting multistage screening rules from online dating activity data.

    Science.gov (United States)

    Bruch, Elizabeth; Feinberg, Fred; Lee, Kee Yeun

    2016-09-20

    This paper presents a statistical framework for harnessing online activity data to better understand how people make decisions. Building on insights from cognitive science and decision theory, we develop a discrete choice model that allows for exploratory behavior and multiple stages of decision making, with different rules enacted at each stage. Critically, the approach can identify if and when people invoke noncompensatory screeners that eliminate large swaths of alternatives from detailed consideration. The model is estimated using deidentified activity data on 1.1 million browsing and writing decisions observed on an online dating site. We find that mate seekers enact screeners ("deal breakers") that encode acceptability cutoffs. A nonparametric account of heterogeneity reveals that, even after controlling for a host of observable attributes, mate evaluation differs across decision stages as well as across identified groupings of men and women. Our statistical framework can be widely applied in analyzing large-scale data on multistage choices, which typify searches for "big ticket" items. PMID:27578870

  1. Screening of antidiabetic and antioxidant activities of medicinal plants

    Institute of Scientific and Technical Information of China (English)

    Amal Bakr Shori

    2015-01-01

    Diabetes is a common metabolic disorder characterized by abnormaly increased plasma glucose levels. Postprandial hyperglycemia plays an essential role in development of type-2 diabetes. Inhibitors of carbohydrate-hydrolyzing enzymes (such as α-glucosidase and α-amylase) offer an effective strategy to regulate/prevent hyperglycemia by controling starch breakdown. Natural α-amylase and α-glucosidase inhibitors, as wel as antioxidants from plant-based sources, offer a source of dietary ingredients that affect human physiological function in order to treat diabetes. Several research studies have investigated the effectiveness of plant-based inhibitors of α-amylase and α-glucosidase, as wel as their antioxidant activity. The aim of this review is to summarize the antidiabetic and antioxidant properties of several medicinal plants around the world. Half inhibitory concentration (IC50,for enzyme suppression) and half effective concentration (EC50, for antioxidant activity) values of less than 500 μg/mL were deifned as the most potent plant-based inhibitors (in vitro) and are expected to provide interesting candidates for herbal treatment of diabetes, as foods, supplements, or reifned drugs.

  2. A Quantitative High-Throughput Screening Data Analysis Pipeline for Activity Profiling.

    Science.gov (United States)

    Huang, Ruili

    2016-01-01

    The US Tox21 program has developed in vitro assays to test large collections of environmental chemicals in a quantitative high-throughput screening (qHTS) format, using triplicate 15-dose titrations to generate over 50 million data points to date. Counter screens are also employed to minimize interferences from non-target-specific assay artifacts, such as compound auto fluorescence and cytotoxicity. New data analysis approaches are needed to integrate these data and characterize the activities observed from these assays. Here, we describe a complete analysis pipeline that evaluates these qHTS data for technical quality in terms of signal reproducibility. We integrate signals from repeated assay runs, primary readouts, and counter screens to produce a final call on on-target compound activity. PMID:27518629

  3. A Quantitative High-Throughput Screening Data Analysis Pipeline for Activity Profiling.

    Science.gov (United States)

    Huang, Ruili

    2016-01-01

    The US Tox21 program has developed in vitro assays to test large collections of environmental chemicals in a quantitative high-throughput screening (qHTS) format, using triplicate 15-dose titrations to generate over 50 million data points to date. Counter screens are also employed to minimize interferences from non-target-specific assay artifacts, such as compound auto fluorescence and cytotoxicity. New data analysis approaches are needed to integrate these data and characterize the activities observed from these assays. Here, we describe a complete analysis pipeline that evaluates these qHTS data for technical quality in terms of signal reproducibility. We integrate signals from repeated assay runs, primary readouts, and counter screens to produce a final call on on-target compound activity.

  4. A consolidated method for screening the endocrine activity of drinking water.

    Science.gov (United States)

    Chevolleau, Sylvie; Debrauwer, Laurent; Stroheker, Thomas; Viglino, Liza; Mourahib, Issam; Meireles, Maria-Helena; Grimaldi, Marina; Balaguer, Patrick; di Gioia, Lodovico

    2016-12-15

    Endocrine activity of drinking water is a matter of growing interest for scientists as well as health authorities. A concentration technique for endocrine activity screening was developed, optimized, and transposed from 200mL to 10L water samples. To avoid any contamination during concentration, the method was developed using exclusively glass, Teflon and stainless steel materials. Any potential losses were tracked using three model radiolabeled molecules, namely BPA, DEHP and 4n-NP. The final method allowed 10L water samples to be concentrated 5000-fold, with good recovery and repeatability. After validation, by concentrating spiked and non-spiked 10L samples of EVIAN natural mineral water, 14 different drinking water samples were concentrated and screened for endocrine disrupting activity using bioluminescent assays. Samples consisting of bottled water, conditioned in various materials (glass, PET) and subjected to different storage conditions, had no hormone-like activities whereas estrogenic activity was found in the filtered tap water. PMID:27451182

  5. PHYTOCHEMICAL SCREENING AND ANTIMICROBIAL ACTIVITY ON THE FRUITS OF HUGONIA MYSTAX L. (LINACEAE

    Directory of Open Access Journals (Sweden)

    A. Vimalavady et al.

    2012-04-01

    Full Text Available An ethnomedicinal plant, Hugonia mystax L., was examined for preliminary phytochemical screening and antimicrobial activity. Preliminary phytochemical screening showed the presence of various classes of secondary metabolites such as flavonoids, phenols, saponins, steroids, tannins and terpenoids. Antimicrobial activity of petroleum ether, chloroform, ethanolic and aqueous fruits extracts showed significant activity against the human pathogens such as Streptococcus pneumoniae causing brain abscesses, pneumonia and septic arthritis; Proteus vulgaris, Pseudomonas aeruginosa causing urinary tract infections and septicaemia; Salmonella typhi causing typhoid fever, Vibrio species causing diarrheal infections and the fungus Candida albicans causes urinary tract infections. The antimicrobial activity of the petroleum ether, chloroform, ethanolic and aqueous fruits extracts showed concentration-dependent activity against all the tested bacteria at various concentrations. Thus the present findings revealed the medicinal potential of H. mystax to develop a drug against various human ailments.

  6. Screen time and physical activity during adolescence: longitudinal effects on obesity in young adulthood

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    Gordon-Larsen Penny

    2007-06-01

    Full Text Available Abstract Background The joint impact of sedentary behavior and physical activity on obesity has not been assessed in a large cohort followed from adolescence to adulthood. Methods Nationally representative longitudinal data from Waves II (1995; mean age: 15.9 and III (2001; mean age: 21.4 of the National Longitudinal Study of Adolescent Health (n = 9,155 were collected. Sex-stratified multivariate logistic regression analysis assessed the odds of obesity associated with Wave II MVPA and screen time, controlling for sociodemographic characteristics and change in MVPA and screen time from Wave II to III. Obesity was defined using body mass index (BMI, kg/m2 International Obesity Task Force cut-points at Wave II and adult cut-points at Wave III (BMI ≥ 30. Results In males, adjusted odds of prevalent obesity was strongly predicted by MVPA bouts [OR (95% CI: OR6 vs. 1 MVPA bouts = 0.50 (0.40, 0.62; OR4 vs. 40 hrs screen time = 0.83 (0.69, 1.00]. In females, greater MVPA bouts and lower screen time correlated with lower prevalent obesity [OR (95% CI: OR6 vs. 1 MVPA bouts = 0.67 (0.49, 0.91; OR4 vs. 40 hrs screen time = 0.67 (0.53, 0.85]. Longitudinally, adolescent screen time hours had a stronger influence on incident obesity in females [OR (95% CI: OR4 vs. 40 hrs = 0.58 (0.43, 0.80] than males [OR (95% CI: OR4 vs. 40 hrs = 0.78 (0.61, 0.99]. Longitudinal activity patterns were not predictive of incident obesity. Conclusion Reducing screen time during adolescence and into adulthood may be a promising strategy for reducing obesity incidence, especially in females.

  7. Antimicrobial activity screening of isolated flavonoids from Azadirachta indica leaves

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    QUDSIA KANWAL

    2011-03-01

    Full Text Available The antimicrobial activities of two flavonoids, namely genistein 7-O-glucoside (1 and (–-epi-catechin (2, isolated from Azadirachta indica A. Juss (neem leaves, were evaluated against five fungal species, viz: Alternaria alternata (Fr. Keissler, Aspergillus fumigatus Fresenius, Aspergillus niger van Tieghem, Macrophomina phaseolina (Tassi Goid. and Penicillium citrii, and four bacterial species, viz. Lactobacillus sp., Escherichia coli, Azospirillium lipoferum and Bacillus sp. Six concentrations, viz. 100, 300, 500, 700, 900 and 1000 ppm of each of the two flavonoids were employed using malt extract agar medium. All the concentrations of both the test compounds significantly suppressed fungal as well as bacterial growth. The highest concentration (1000 ppm of both fractions 1 and 2 reduced the growth of the different test fungal species by 83–99 % and 82–95 %, respectively. Compound 1 was highly effective against Lactobacillus sp., against which its various concentrations reduced the bacterial growth by 52–99.8 %. Compound 2 was highly effective against A. lipoferum and Bacillus sp., resulting in 94–100 % and 73–99% reduction in bacterial growth, respectively.

  8. SCREENING OF ANTIMICROBIAL, CYTOTOXIC AND PESTICIDAL ACTIVITIES OF COCCINIA GRANDIS (L. VOIGT

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    Md. Faruk Hasan

    2016-06-01

    Full Text Available This study was undertaken to assess the antibacterial, antifungal, cytotoxic and pesticidal activities of Coccinia grandis roots extract. The antimicrobial activity was evaluated using disc diffusion method against some pathogenic microorganisms. Cytotoxicity was determined using brine shrimp lethality bioassay method. The plant extract was screened for pesticidal activity towards Sitophilus oryzae adults. Minimum inhibitory concentration (MIC was also studied against test organisms, using serial dilution technique to determine the antibacterial potency. In antibacterial screening, large inhibition zones were observed against the tested gram-positive (Bacillus subtilis, Sarcina lutea and Stapphylococcus aureus and gram-negative (Salmonella typhi and Shigella dysenteriae bacteria. In antifungal screening, the extract showed moderate antifungal activities against the tested fungi (Candida albicans and Colletotrichum falcatum. In cytotoxicity activity test, LC50 (lethal concentration, 50% of the extract against brine shrimp nauplii was 15.00µg/ml. The plant extract also showed moderate pesticidal activities towards S. oryzae adults. These results suggested that the plant extract has significant antibacterial activity against the tested bacteria, moderate antifungal, cytotoxic and pesticidal activity towards the tested fungi, brine shrimp nauplii and S. oryzae adults, respectively.

  9. How parents can affect excessive spending of time on screen-based activities

    NARCIS (Netherlands)

    Brindova, Daniela; Pavelka, Jan; Sevcikova, Anna; Zezula, Ivan; van Dijk, Jitse P.; Reijneveld, Sijmen A.; Geckova, Andrea Madarasova

    2014-01-01

    Background: The aim of this study is to explore the association between family-related factors and excessive time spent on screen-based activities among school-aged children. Methods: A cross-sectional survey using the methodology of the Health Behaviour in School-aged Children study was performed i

  10. Agar composition affects in vitro screening of biocontrol activity of antagonistic microorganisms

    NARCIS (Netherlands)

    Bosmans, Lien; De Bruijn, I.; de Mot, Rene; Readers, Hans; Lievens, Bart

    2016-01-01

    Agar-based screening assays are the method of choice when evaluating antagonistic potential of bacterial biocontrol-candidates against pathogens.Weshowed thatwhen using the samemedium, but different agar compositions, the activity of a bacterial antagonist against Agrobacteriumwas strongly affected.

  11. Screening of Plant Extracts for Antioxidant Activity: a Comparative Study on Three Testing Methods

    NARCIS (Netherlands)

    Koleva, I.; Beek, van T.A.; Linssen, J.P.H.; Groot, de Æ.; Evstatieva, L.N.

    2002-01-01

    Three methods widely employed in the evaluation of antioxidant activity, namely 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging method, static headspace gas chromatography (HS-GC) and -carotene bleaching test (BCBT), have been compared with regard to their application in the screening of pla

  12. A Pipeline for Screening Small Molecules with Growth Inhibitory Activity against Burkholderia cenocepacia.

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    Carrie Selin

    Full Text Available Infections with the bacteria Burkholderia cepacia complex (Bcc are very difficult to eradicate in cystic fibrosis patients due the intrinsic resistance of Bcc to most available antibiotics and the emergence of multiple antibiotic resistant strains during antibiotic treatment. In this work, we used a whole-cell based assay to screen a diverse collection of small molecules for growth inhibitors of a relevant strain of Bcc, B. cenocepacia K56-2. The primary screen used bacterial growth in 96-well plate format and identified 206 primary actives among 30,259 compounds. From 100 compounds with no previous record of antibacterial activity secondary screening and data mining selected a total of Bce bioactives that were further analyzed. An experimental pipeline, evaluating in vitro antibacterial and antibiofilm activity, toxicity and in vivo antibacterial activity using C. elegans was used for prioritizing compounds with better chances to be further investigated as potential Bcc antibacterial drugs. This high throughput screen, along with the in vitro and in vivo analysis highlights the utility of this experimental method to quickly identify bioactives as a starting point of antibacterial drug discovery.

  13. A Pipeline for Screening Small Molecules with Growth Inhibitory Activity against Burkholderia cenocepacia.

    Science.gov (United States)

    Selin, Carrie; Stietz, Maria S; Blanchard, Jan E; Gehrke, Sebastian S; Bernard, Sylvain; Hall, Dennis G; Brown, Eric D; Cardona, Silvia T

    2015-01-01

    Infections with the bacteria Burkholderia cepacia complex (Bcc) are very difficult to eradicate in cystic fibrosis patients due the intrinsic resistance of Bcc to most available antibiotics and the emergence of multiple antibiotic resistant strains during antibiotic treatment. In this work, we used a whole-cell based assay to screen a diverse collection of small molecules for growth inhibitors of a relevant strain of Bcc, B. cenocepacia K56-2. The primary screen used bacterial growth in 96-well plate format and identified 206 primary actives among 30,259 compounds. From 100 compounds with no previous record of antibacterial activity secondary screening and data mining selected a total of Bce bioactives that were further analyzed. An experimental pipeline, evaluating in vitro antibacterial and antibiofilm activity, toxicity and in vivo antibacterial activity using C. elegans was used for prioritizing compounds with better chances to be further investigated as potential Bcc antibacterial drugs. This high throughput screen, along with the in vitro and in vivo analysis highlights the utility of this experimental method to quickly identify bioactives as a starting point of antibacterial drug discovery. PMID:26053039

  14. Phyto chemical Screening, Antibacterial, Antifungal and Anthelmintic Activity of Morinda citrifolia stem

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    Dr. D. Gopala Krishna

    2013-05-01

    Full Text Available In the present study, the Petroleum Ether and Alcoholic extract of Morinda citrifolia L. (Noni stem were subjected to preliminary screening for Antimicrobial and Aanthelmintic activity. The alcoholic extract exhibited significant Anti bacterial, Antifungal activity, comparable to the standard drug Tetracycline. The Petroleum Ether and Alcoholic extract were evaluated for Anthelmintic activity on adult Indian Earthworms, ‘Pheretima posithuma’. The Alcoholic extract produced more significant Anthelmintic activity than Petroleum ether extract and the activities are comparable with the reference drug Piperazine citrate

  15. Phytochemical screening and antioxidant activity of ethanol extract of Tithonia diversifolia (Hemsl) A. Gray dry flowers

    Institute of Scientific and Technical Information of China (English)

    Robson Miranda da Gama; Marcelo Guimares; Luiz Carlos de Abreu; Jos Armando-Junior

    2014-01-01

    Objective:To evaluate the antioxidant activity of extracts of dried flowers of Tithonia diversifolia (Hemsl) A. Gray (T. diversifolia) dry flower-a shrubby plant belonging to the Asteraceae family and very common in Brazil, providing data to help prevent premature aging skin. Methods: The tests of phytochemical screening included total phenols, tannins, flavonoids, alkaloids and saponins. The active antioxidant was determined by 2,2-diphenyl-1-picryl-hydrazyl method. Results: The phytochemical screening of T. diversifolia dry flowers revealed the presence of phenolic compounds (tannins, flavonoids and total phenols), while alkaloids and saponins were not detected. The IC50 values showed a strong antioxidant activity of the plant extracts. Conclusions: Therefore, this study suggests the possibility of using dry flowers extracts of T. diversifolia for the prevention of cell aging, as was shown to have significant antioxidant activity.

  16. Small-molecule activators of insulin-degrading enzyme discovered through high-throughput compound screening.

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    Christelle Cabrol

    Full Text Available BACKGROUND: Hypocatabolism of the amyloid beta-protein (Abeta by insulin-degrading enzyme (IDE is implicated in the pathogenesis of Alzheimer disease (AD, making pharmacological activation of IDE an attractive therapeutic strategy. However, it has not been established whether the proteolytic activity of IDE can be enhanced by drug-like compounds. METHODOLOGY/PRINCIPAL FINDINGS: Based on the finding that ATP and other nucleotide polyphosphates modulate IDE activity at physiological concentrations, we conducted parallel high-throughput screening campaigns in the absence or presence of ATP and identified two compounds--designated Ia1 and Ia2--that significantly stimulate IDE proteolytic activity. Both compounds were found to interfere with the crosslinking of a photoaffinity ATP analogue to IDE, suggesting that they interact with a bona fide ATP-binding domain within IDE. Unexpectedly, we observed highly synergistic activation effects when the activity of Ia1 or Ia2 was tested in the presence of ATP, a finding that has implications for the mechanisms underlying ATP-mediated activation of IDE. Notably, Ia1 and Ia2 activated the degradation of Abeta by approximately 700% and approximately 400%, respectively, albeit only when Abeta was presented in a mixture also containing shorter substrates. CONCLUSIONS/SIGNIFICANCE: This study describes the first examples of synthetic small-molecule activators of IDE, showing that pharmacological activation of this important protease with drug-like compounds is achievable. These novel activators help to establish the putative ATP-binding domain as a key modulator of IDE proteolytic activity and offer new insights into the modulatory action of ATP. Several larger lessons abstracted from this screen will help inform the design of future screening campaigns and facilitate the eventual development of IDE activators with therapeutic utility.

  17. New Approach for High-Throughput Screening of Drug Activity on Plasmodium Liver Stages

    OpenAIRE

    Gego, Audrey; Silvie, Olivier; Franetich, Jean-François; Farhati, Khemaïs; Hannoun, Laurent; Luty, Adrian J. F.; Robert W Sauerwein; Boucheix, Claude; Rubinstein, Eric; Mazier, Dominique

    2006-01-01

    Plasmodium liver stages represent potential targets for antimalarial prophylactic drugs. Nevertheless, there is a lack of molecules active on these stages. We have now developed a new approach for the high-throughput screening of drug activity on Plasmodium liver stages in vitro, based on an infrared fluorescence scanning system. This method allowed us to count automatically and rapidly Plasmodium-infected hepatocytes, using different hepatic cells and different Plasmodium species, including ...

  18. Screening vaccine formulations for biological activity using fresh human whole blood

    OpenAIRE

    Brookes, RH; Hakimi, J; Ha, Y; Aboutorabian, S; Ausar, SF; Hasija, M; Smith, SG; Todryk, SM; Dockrell, HM; Rahman, N

    2014-01-01

    Understanding the relevant biological activity of any pharmaceutical formulation destined for human use is crucial. For vaccine-based formulations, activity must reflect the expected immune response, while for non-vaccine therapeutic agents, such as monoclonal antibodies, a lack of immune response to the formulation is desired. During early formulation development, various biochemical and biophysical characteristics can be monitored in a high-throughput screening (HTS) format. However, it rem...

  19. In vitro Antimicrobial Activity and Phytochemical Screening of Clematis Species Indigenous to Ethiopia

    OpenAIRE

    S Hawaze; Deti, H.; Suleman, S.

    2012-01-01

    The leaves extracts of two indigenous plants of Ethiopia: Clematis longicauda steud ex A. Rich. and Clematis burgensis Engl. are used in Southwestern Ethiopia to treat otorrhoea and eczema. Antimicrobial activity and MIC of crude extracts were determined by disk diffusion and broth dilution. Phytochemical screening was performed on the extracts. The methanol and petroleum ether extracts of both plants showed antibacterial and antifungal activity. Sensitivity of reference strains was concentra...

  20. Screening of Various Botanical Extracts for Antioxidant Activity Using DPPH Free Radical Method

    OpenAIRE

    Waqas, Muhammad Khurram; Saqib, Najam-Us; Rashid, Saeed-ur; Shah, Pervaiz Akhtar; Akhtar, Naveed; Murtaza, Ghulam

    2013-01-01

    Aiming at the exploration of herbal use by society, crude extracts of the seeds of some commonly used medicinal plants (Vitis vinifera, Tamarindus indica and Glycin max) were screened for their free radical scavenging properties using ascorbic acid as standard antioxidant. Free radical scavenging activity was evaluated using 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical. The overall antioxidant activity of grape seeds (Vitis vinifera) was the strongest, followed in descending order by soy...

  1. Isolation of actinomycetes from mangrove and estuarine sediments of Cochin and screening for antimicrobial activity

    Institute of Scientific and Technical Information of China (English)

    Emilda Rosmine

    2016-01-01

    Objective:To isolate and screen actinomycetes for antimicrobial activity from mangroves and estuarine soil samples of Cochin. Methods: In the present study, sediment samples collected from mangroves and various stations of Cochin estuary were pretreated and actinomycetes were isolated on different selective media. The isolates were screened for antibiotic activity by following disc diffusion assay (Kirby-Bauer method) against human pathogens, fish pathogens and Gram-positive bacteria. The isolates were identified based on their morphology. Results:Only 2 actinomycete isolates (ER7and ER10) of the 50 isolates screened had antimicrobial activities against one or more pathogens tested. ER7 isolate showed higher antimicrobial activity as compared to that of ER10 isolate. The maximum inhibition zone of crude extract from ER7 was 16.7 mm. The methanol extract of ER7 showed antimicrobial activity against all the pathogens tested with a maximum zone of 21.0 mm. The isolates with antimicrobial activity were found to belong to the genusStreptomyces. Conclusions:There is no significant report on bioactive actinomycetes from the present study areas. Potent antibiotics from the selected isolates could contribute to fight against several human and fish diseases. Further purification, structural elucidation and characterization are recommended to know the quality, novelty and commercial value of these antibiotics. Hence, the mangroves and estuary of Kochi show great promise for the discovery of bioactive actinomycetes.

  2. Associations of parental influences with physical activity and screen time among young children: a systematic review.

    Science.gov (United States)

    Xu, Huilan; Wen, Li Ming; Rissel, Chris

    2015-01-01

    Parents play a critical role in developing and shaping their children's physical activity (PA) and sedentary behaviours, particularly in the early years of life. The aim of this systematic review is to identify current literature investigating associations of parental influences with both PA and screen time in young children. This systematic review was conducted in November 2013 using 6 electronic databases covering research literature from January 1998 to November 2013. Thirty articles that met inclusion criteria were identified. These studies covered five important aspects of parenting: (1) parenting practices; (2) parents' role modelling; (3) parental perceptions of children's PA and screen viewing behaviours; (4) parental self-efficacy; and (5) general parenting style. Findings suggest that parents' encouragement and support can increase children's PA, and reducing parents' own screen time can lead to decreased child screen time. Improving parenting practices, parental self-efficacy or changing parenting style may also be promising approaches to increasing PA time and decreasing screen time of young children.

  3. Associations of Parental Influences with Physical Activity and Screen Time among Young Children: A Systematic Review

    Directory of Open Access Journals (Sweden)

    Huilan Xu

    2015-01-01

    Full Text Available Parents play a critical role in developing and shaping their children’s physical activity (PA and sedentary behaviours, particularly in the early years of life. The aim of this systematic review is to identify current literature investigating associations of parental influences with both PA and screen time in young children. This systematic review was conducted in November 2013 using 6 electronic databases covering research literature from January 1998 to November 2013. Thirty articles that met inclusion criteria were identified. These studies covered five important aspects of parenting: (1 parenting practices; (2 parents’ role modelling; (3 parental perceptions of children’s PA and screen viewing behaviours; (4 parental self-efficacy; and (5 general parenting style. Findings suggest that parents’ encouragement and support can increase children’s PA, and reducing parents’ own screen time can lead to decreased child screen time. Improving parenting practices, parental self-efficacy or changing parenting style may also be promising approaches to increasing PA time and decreasing screen time of young children.

  4. CETSA screening identifies known and novel thymidylate synthase inhibitors and slow intracellular activation of 5-fluorouracil

    Science.gov (United States)

    Almqvist, Helena; Axelsson, Hanna; Jafari, Rozbeh; Dan, Chen; Mateus, André; Haraldsson, Martin; Larsson, Andreas; Molina, Daniel Martinez; Artursson, Per; Lundbäck, Thomas; Nordlund, Pär

    2016-03-01

    Target engagement is a critical factor for therapeutic efficacy. Assessment of compound binding to native target proteins in live cells is therefore highly desirable in all stages of drug discovery. We report here the first compound library screen based on biophysical measurements of intracellular target binding, exemplified by human thymidylate synthase (TS). The screen selected accurately for all the tested known drugs acting on TS. We also identified TS inhibitors with novel chemistry and marketed drugs that were not previously known to target TS, including the DNA methyltransferase inhibitor decitabine. By following the cellular uptake and enzymatic conversion of known drugs we correlated the appearance of active metabolites over time with intracellular target engagement. These data distinguished a much slower activation of 5-fluorouracil when compared with nucleoside-based drugs. The approach establishes efficient means to associate drug uptake and activation with target binding during drug discovery.

  5. Active Learning Strategies for Phenotypic Profiling of High-Content Screens.

    Science.gov (United States)

    Smith, Kevin; Horvath, Peter

    2014-06-01

    High-content screening is a powerful method to discover new drugs and carry out basic biological research. Increasingly, high-content screens have come to rely on supervised machine learning (SML) to perform automatic phenotypic classification as an essential step of the analysis. However, this comes at a cost, namely, the labeled examples required to train the predictive model. Classification performance increases with the number of labeled examples, and because labeling examples demands time from an expert, the training process represents a significant time investment. Active learning strategies attempt to overcome this bottleneck by presenting the most relevant examples to the annotator, thereby achieving high accuracy while minimizing the cost of obtaining labeled data. In this article, we investigate the impact of active learning on single-cell-based phenotype recognition, using data from three large-scale RNA interference high-content screens representing diverse phenotypic profiling problems. We consider several combinations of active learning strategies and popular SML methods. Our results show that active learning significantly reduces the time cost and can be used to reveal the same phenotypic targets identified using SML. We also identify combinations of active learning strategies and SML methods which perform better than others on the phenotypic profiling problems we studied.

  6. Screening of some traditionally used medicinal plants for potential antibacterial activity

    Directory of Open Access Journals (Sweden)

    Parekh Jigna

    2006-01-01

    Full Text Available In the present work an attempt has been made to carry out screening for the preliminary antibacterial activity of different plants used in Indian folk medicine. The aim of the study was to select an active plant extract which may be useful in developing new lead compounds to combat deadly diseases. Twelve plants were selected for preliminary screening for their antibacterial potentiality, viz., Abutilon indicum L., Acorous calamus L., Ammania baccifera L., Argyrea nervosa Burm. F., Bauhinia variegata L., Crataeva religiosa Forst., Hedychium spicatum L., Holarrhena antidysenterica L., Piper nigrum L., Plumbago zeylanica L., Psoralea corylifolia L., Saussurea lappa Costus. The antibacterial activity was done by both agar disc diffusion method and agar well diffusion method against five bacterial strains, viz., Bacillus cereus, Staphylococcus aureus, Klebsiella pneumoniae, Escherichia coli, Pseudomonas pseudoalcaligenes . The plant material was extracted with distilled water (aqueous and methanol. The preliminary screening experiment revealed that methanol extracts were more potent than the aqueous extracts. The plant extracts were more active against gram-positive bacteria than gram-negative bacteria. The most susceptible bacteria were K. pneumoniae and the most resistant bacteria were E. coli . Bauhinia variegata L. exhibited remarkable antibacterial activity.

  7. Screening of plants containing Naja naja siamensis cobra venom inhibitory activity using modified ELISA technique.

    Science.gov (United States)

    Daduang, Sakda; Sattayasai, Nison; Sattayasai, Jintana; Tophrom, Pattara; Thammathaworn, Achra; Chaveerach, Arunrat; Konkchaiyaphum, Monruedee

    2005-06-15

    Enzyme-linked immunosorbent assay (ELISA) has been modified for screening plants with antagonistic activity to Naja naja siamensis cobra venom. Aqueous extracts from plants were investigated for their inhibitory effects on the binding of anti-cobra venom antibody to antigen, cobra venom, fixed onto 96-well microtiter plates. Ingredients in extracts were allowed to react with immobilized venom before the subsequent addition of antivenom antibody. Venom components affected by exposure to the extracts, unable to interact with their specific antibody, were predicted to be unable to bind to their native destinations or natural receptors. Curcuma cf. zedoaria, an old Thai medicinal plant, showed clear inhibitory activity in the ELISA test. Neurotoxin and protein degradative enzymes, major components in venom, were identified as targets of this extract in Western immunoblotting analysis. Ingredients in the extract showed high affinity to the toxin in competition assay by immunoprecipitation. The extract attenuated toxin activity by extending contraction time of diaphragm muscle after envenomation and had a potency to protect cellular proteins from venom degradative enzymes. Curcuma parviflora, with less activity in ELISA, exhibited acceptable results in two experiments but negative results in two experiments, whereas Curcuma longa, having low activity in the ELISA test, never showed any favorable results. Screening of 36 samples could classify plants into an inhibition range of 0 to 86%. This modified ELISA is recommended as a preliminary screening method for inhibitors with a large number of samples.

  8. Population-based cohort study of anti-infective medication use before and after the onset of type 1 diabetes in children and adolescents

    NARCIS (Netherlands)

    Fazeli Farsani, Soulmaz; Souverein, Patrick C; van der Vorst, Marja M J; Knibbe, Catherijne A J; de Boer, Anthonius; Mantel-Teeuwisse, Aukje K

    2014-01-01

    A population-based cohort study was conducted in the Dutch PHARMO database to investigate prevalence and patterns of anti-infective medication use in children and adolescents with type 1 diabetes (T1D) before and after the onset of this disease. All patients <19 years with at least 2 insulin prescri

  9. An exposure:activity profiling method for interpreting high-throughput screening data for estrogenic activity--proof of concept.

    Science.gov (United States)

    Becker, Richard A; Friedman, Katie Paul; Simon, Ted W; Marty, M Sue; Patlewicz, Grace; Rowlands, J Craig

    2015-04-01

    Rapid high throughput in vitro screening (HTS) assays are now available for characterizing dose-responses in assays that have been selected for their sensitivity in detecting estrogen-related endpoints. For example, EPA's ToxCast™ program recently released endocrine assay results for more than 1800 substances and the interagency Tox21 consortium is in the process of releasing data for approximately 10,000 chemicals. But such activity measurements alone fall short for the purposes of priority setting or screening because the relevant exposure context is not considered. Here, we extend the method of exposure:activity profiling by calculating the exposure:activity ratios (EARs) using human exposure estimates and AC50 values for a range of chemicals tested in a suite of seven estrogenic assays in ToxCast™ and Tox21. To provide additional context, relative estrogenic exposure:activity quotients (REEAQ) were derived by comparing chemical-specific EARs to the EAR of the ubiquitous dietary phytoestrogen, genistein (GEN). Although the activity of a substance in HTS-endocrine assays is not a measure of health hazard or risk, understanding how such a dose compares to human exposures provides a valuable additional metric that can be used in decision-making; substances with small EARs and REEAQs would indicate low priority for further endocrine screening or testing. PMID:25656492

  10. Screening a Commercial Library of Pharmacologically Active Small Molecules against Staphylococcus aureus Biofilms.

    Science.gov (United States)

    Torres, Nelson S; Abercrombie, Johnathan J; Srinivasan, Anand; Lopez-Ribot, Jose L; Ramasubramanian, Anand K; Leung, Kai P

    2016-10-01

    It is now well established that bacterial infections are often associated with biofilm phenotypes that demonstrate increased resistance to common antimicrobials. Further, due to the collective attrition of new antibiotic development programs by the pharmaceutical industries, drug repurposing is an attractive alternative. In this work, we screened 1,280 existing commercially available drugs in the Prestwick Chemical Library, some with previously unknown antimicrobial activity, against Staphylococcus aureus, one of the commonly encountered causative pathogens of burn and wound infections. From the primary screen of the entire Prestwick Chemical Library at a fixed concentration of 10 μM, 104 drugs were found to be effective against planktonic S. aureus strains, and not surprisingly, these were mostly antimicrobials and antiseptics. The activity of 18 selected repurposing candidates, that is, drugs that show antimicrobial activity that are not already considered antimicrobials, observed in the primary screen was confirmed in dose-response experiments. Finally, a subset of nine of these drug candidates was tested against preformed biofilms of S. aureus We found that three of these drugs, niclosamide, carmofur, and auranofin, possessed antimicrobial activity against preformed biofilms, making them attractive candidates for repurposing as novel antibiofilm therapies. PMID:27401577

  11. A new versatile microarray-based method for high throughput screening of carbohydrate-active enzymes.

    Science.gov (United States)

    Vidal-Melgosa, Silvia; Pedersen, Henriette L; Schückel, Julia; Arnal, Grégory; Dumon, Claire; Amby, Daniel B; Monrad, Rune Nygaard; Westereng, Bjørge; Willats, William G T

    2015-04-01

    Carbohydrate-active enzymes have multiple biological roles and industrial applications. Advances in genome and transcriptome sequencing together with associated bioinformatics tools have identified vast numbers of putative carbohydrate-degrading and -modifying enzymes including glycoside hydrolases and lytic polysaccharide monooxygenases. However, there is a paucity of methods for rapidly screening the activities of these enzymes. By combining the multiplexing capacity of carbohydrate microarrays with the specificity of molecular probes, we have developed a sensitive, high throughput, and versatile semiquantitative enzyme screening technique that requires low amounts of enzyme and substrate. The method can be used to assess the activities of single enzymes, enzyme mixtures, and crude culture broths against single substrates, substrate mixtures, and biomass samples. Moreover, we show that the technique can be used to analyze both endo-acting and exo-acting glycoside hydrolases, polysaccharide lyases, carbohydrate esterases, and lytic polysaccharide monooxygenases. We demonstrate the potential of the technique by identifying the substrate specificities of purified uncharacterized enzymes and by screening enzyme activities from fungal culture broths.

  12. Screening a Commercial Library of Pharmacologically Active Small Molecules against Staphylococcus aureus Biofilms.

    Science.gov (United States)

    Torres, Nelson S; Abercrombie, Johnathan J; Srinivasan, Anand; Lopez-Ribot, Jose L; Ramasubramanian, Anand K; Leung, Kai P

    2016-10-01

    It is now well established that bacterial infections are often associated with biofilm phenotypes that demonstrate increased resistance to common antimicrobials. Further, due to the collective attrition of new antibiotic development programs by the pharmaceutical industries, drug repurposing is an attractive alternative. In this work, we screened 1,280 existing commercially available drugs in the Prestwick Chemical Library, some with previously unknown antimicrobial activity, against Staphylococcus aureus, one of the commonly encountered causative pathogens of burn and wound infections. From the primary screen of the entire Prestwick Chemical Library at a fixed concentration of 10 μM, 104 drugs were found to be effective against planktonic S. aureus strains, and not surprisingly, these were mostly antimicrobials and antiseptics. The activity of 18 selected repurposing candidates, that is, drugs that show antimicrobial activity that are not already considered antimicrobials, observed in the primary screen was confirmed in dose-response experiments. Finally, a subset of nine of these drug candidates was tested against preformed biofilms of S. aureus We found that three of these drugs, niclosamide, carmofur, and auranofin, possessed antimicrobial activity against preformed biofilms, making them attractive candidates for repurposing as novel antibiofilm therapies.

  13. Rapid ester biosynthesis screening reveals a high activity alcohol-O-acyltransferase (AATase) from tomato fruit.

    Science.gov (United States)

    Lin, Jyun-Liang; Zhu, Jie; Wheeldon, Ian

    2016-05-01

    Ethyl and acetate esters are naturally produced in various yeasts, plants, and bacteria. The biosynthetic pathways that produce these esters share a common reaction step, the condensation of acetyl/acyl-CoA with an alcohol by alcohol-O-acetyl/acyltransferase (AATase). Recent metabolic engineering efforts exploit AATase activity to produce fatty acid ethyl esters as potential diesel fuel replacements as well as short- and medium-chain volatile esters as fragrance and flavor compounds. These efforts have been limited by the lack of a rapid screen to quantify ester biosynthesis. Enzyme engineering efforts have also been limited by the lack of a high throughput screen for AATase activity. Here, we developed a high throughput assay for AATase activity and used this assay to discover a high activity AATase from tomato fruit, Solanum lycopersicum (Atf-S.l). Atf1-S.l exhibited broad specificity towards acyl-CoAs with chain length from C4 to C10 and was specific towards 1-pentanol. The AATase screen also revealed new acyl-CoA substrate specificities for Atf1, Atf2, Eht1, and Eeb1 from Saccharomyces cerevisiae, and Atf-C.m from melon fruit, Cucumis melo, thus increasing the pool of characterized AATases that can be used in ester biosynthesis of ester-based fragrance and flavor compounds as well as fatty acid ethyl ester biofuels. PMID:26814045

  14. PRE-CLINICAL SCREENING OF INDIGENOUS MEDICINAL PLANT PHYLLANTHUS AMARUS FOR ITS ANALGESIC ACTIVITY

    Directory of Open Access Journals (Sweden)

    Sundeep Hegde K

    2014-11-01

    Full Text Available Background: Phyllanthus amarus aqueous extract was investigated for its central and peripheral analgesic activities. Objectives: To evaluate the central and peripheral analgesic activities of aqueous extract of Phyllanthus amarus. Materials and Methods: The aqueous extract of Phyllanthus amarus was prepared using soxhlet apparatus. An in vivo study using Swiss albino mice was done to screen the central and peripheral analgesic activity of P.amarus extract. The extract was administered at a dose of 100 mg/kg body weight I.P. The peripheral analgesic activity was assessed using acetic acid induced writhing test.The central analgesic activity was assessed using Eddy’s hot plate apparatus. Results: The aqueous extract of P.amarus showed significant (p<0.05 peripheral and central analgesic activity.Conclusion: This study demonstrated that P.amarus aqueous extract exhibited significant analgesic activities.

  15. SCREENING OF SECONDARY METABOLITES AND ANTIBACTERIAL ACTIVITY OF ACACIA CONCINNA LEAVES

    Directory of Open Access Journals (Sweden)

    Xavier Vergeese raja

    2012-10-01

    Full Text Available The preliminary phytochemical study and in vitro antibacterial activity of the leaf extracts of Acacia concinna having ethno medicinal uses were investigated. The preliminary phytochemical analysis of the extracts revealed the presence of phenol, tannin, fat and fixed oil, flavanoids, saponin and quinone. The extracts were subjected for screening of in vitro antibacterial activity against various pathogens at the concentrations of 500 and 250 µg/ml by well diffusion assay method. The results of antibacterial activity revealed that all the extract showed good inhibitory activity against all the tested pathogens and the chloroform extract showed comparative by better activity than the other extracts against S.pyogens and s. aureus. The activities of the extract were compared with standard antibiotics. These results indicate that A. concinna leaves possesses potential broad spectrum antibacterial activity.

  16. Screening of various botanical extracts for antioxidant activity using DPPH free radical method.

    Science.gov (United States)

    Waqas, Muhammad Khurram; Saqib, Najam-Us; Rashid, Saeed-Ur; Shah, Pervaiz Akhtar; Akhtar, Naveed; Murtaza, Ghulam

    2013-01-01

    Aiming at the exploration of herbal use by society, crude extracts of the seeds of some commonly used medicinal plants (Vitis vinifera, Tamarindus indica and Glycin max) were screened for their free radical scavenging properties using ascorbic acid as standard antioxidant. Free radical scavenging activity was evaluated using 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical. The overall antioxidant activity of grape seeds (Vitis vinifera) was the strongest, followed in descending order by soybean (Glycin max) and tamarind (Tamarindus indica). The seeds extract of Vitis vinifera, Glycin max and Tamarindus indica showed 85.61%, 83.45% and 79.26%, DPPH scavenging activity respectively.

  17. Screening of Endophytic Fungi from Chlorophyta and Phaeophyta for Antibacterial Activity

    Science.gov (United States)

    Rahaweman, A. C.; Pamungkas, J.; Madduppa, H.; Thoms, C.; Tarman, K.

    2016-01-01

    Chlorophyta and Phaeophyta macroalgae are important sources of secondary metabolites with pharmaceutically relevant antibacterial, antifungal and antiviral bioactivities. Oftentimes, these algae-derived compounds are, in fact, produced by endophytic fungi living inside the macroalgal tissue. Numerous studies have shown that endophytic fungi can produce a broad range of active metabolites such as terpenes, alkaloids, and quinones. The aim of the present study was to screen fungal strains isolated from a variety of Caulerpa spp., Halimeda spp., and Sargassum spp. for antibacterial activity against Staphylococcus aureus and Escherichia coli. Thirteen morphologically different isolates were tested. Two of them showed pronounced activity against S. aureus in agar diffusion assays.

  18. Short Communication: Antimycotic activity and phytochemical screening of fungal endophytes associated with Santalum album

    Directory of Open Access Journals (Sweden)

    ASHWANI TAPWAL

    2016-05-01

    Full Text Available Abstract. Tapwal A, Pradhan S, Chandra S, Rashmi. 2016. Antimycotic activity and phytochemical screening of fungal endophytes associated with Santalum album. Nusantara Bioscience 8: 14-17. The heartwood of Santalum album constitutes the central part of the tree is valued for its fragrance. The wood and oil are utilized in medicine. Sandalwood oil is extensively used in perfumery, cosmetics, aromatherapy and pharmaceutical industry. The endophytic microorganisms inhabiting the plant tissues are expected to mimic some of the metabolites of its host. This study was aimed to isolate and screen the fungal endophytes inhabiting the Santalum album for antimicrobial activity and for the presence of important phytochemicals. Five fungal endophytes isolated from different parts of S. album have exhibited antimicrobial potential against Fusarium oxysporum in the range of 5.0-40.4%. The isolated endophytic fungi also indicated the presence of alkaloids, phenolics and tannins, flavonoids, carbohydrates and glycosides, terpenoids, amino acids and proteins.

  19. Display technology on filamentous phage in the search for anti-infective biological agents

    Directory of Open Access Journals (Sweden)

    Nelson Santiago Vispo

    2016-01-01

    Full Text Available Introduction: The causes of antibiotic resistance are complex. The phage display technology has been used mainly to produce monoclonal antibodies (MAbs and peptides directed against cancer or inflammatory disease targets. Today, this technology is recognized as a powerful tool for selecting novel peptides and antibodies that can bind to a wide range of antigens, ranging from whole cells to proteins and lipid targets. In this review, we highlight research that exploits the phage display technology to discover new drugs against infectious diseases, with a focus on antimicrobial peptides and antibodies. Methods: Basic and recent literature review was made, mainly focused on general aspects of phage display technology and the application in the search of new peptides or antibodies of pharmaceutical use to combat the infectious diseases transmitted by bacteria and virus. Results: Updated information on the selected topics is shown, with a guiding and practical approach aimed at researchers in the field of molecular biology to continue deepening the technology with special emphasis in the applications that have been developed in Cuba. Conclusions: Advances in methods of screening, manufacturing, and humanization technologies show that phage display technology can significantly contribute in the fight against clinically important pathogens.

  20. Short Communication: Antimycotic activity and phytochemical screening of fungal endophytes associated with Santalum album

    OpenAIRE

    ASHWANI TAPWAL; SWETA PRADHAN; SURESH CHANDRA; RASHMI

    2016-01-01

    Abstract. Tapwal A, Pradhan S, Chandra S, Rashmi. 2016. Antimycotic activity and phytochemical screening of fungal endophytes associated with Santalum album. Nusantara Bioscience 8: 14-17. The heartwood of Santalum album constitutes the central part of the tree is valued for its fragrance. The wood and oil are utilized in medicine. Sandalwood oil is extensively used in perfumery, cosmetics, aromatherapy and pharmaceutical industry. The endophytic microorganisms inhabiting the plant tissues ar...

  1. Preliminary phytochemical screening and In vitro antioxidant activities of the aqueous extract of Helichrysum longifolium DC

    OpenAIRE

    Okoh Anthony I; Aiyegoro Olayinka A

    2010-01-01

    Abstract Background Many oxidative stress related diseases are as a result of accumulation of free radicals in the body. A lot of researches are going on worldwide directed towards finding natural antioxidants of plants origins. The aims of this study were to evaluate in vitro antioxidant activities and to screen for phytochemical constituents of Helichrysum longifolium DC. [Family Asteraceae] aqueous crude extract. Methods We assessed the antioxidant potential and phytochemical constituents ...

  2. Phytochemical screening and antibacterial activity of aqueous leaf extract of Punica granatum

    OpenAIRE

    Manoj Kumar; Sukumar Dandapat; Manoranjan Prasad Sinha

    2015-01-01

    In the present study the leaves of Punica granatum were subjected to phytochemical screening and the impact of the leaf extract of Punica granatum was tested against Bacillus subtilis, Staphylococcus aureus and Salmonella typhi. The phytochemical analysis revealed the presence of various phytochemicals such as alkaloids, tannins, phenols, flavonoid and saponins. Agar disk diffusion method was employed to test the antibacterial activity and the result showed that the aquesous leaf extract o...

  3. LASSO-ligand activity by surface similarity order: a new tool for ligand based virtual screening.

    Science.gov (United States)

    Reid, Darryl; Sadjad, Bashir S; Zsoldos, Zsolt; Simon, Aniko

    2008-01-01

    Virtual Ligand Screening (VLS) has become an integral part of the drug discovery process for many pharmaceutical companies. Ligand similarity searches provide a very powerful method of screening large databases of ligands to identify possible hits. If these hits belong to new chemotypes the method is deemed even more successful. eHiTS LASSO uses a new interacting surface point types (ISPT) molecular descriptor that is generated from the 3D structure of the ligand, but unlike most 3D descriptors it is conformation independent. Combined with a neural network machine learning technique, LASSO screens molecular databases at an ultra fast speed of 1 million structures in under 1 min on a standard PC. The results obtained from eHiTS LASSO trained on relatively small training sets of just 2, 4 or 8 actives are presented using the diverse directory of useful decoys (DUD) dataset. It is shown that over a wide range of receptor families, eHiTS LASSO is consistently able to enrich screened databases and provides scaffold hopping ability.

  4. Screening vaccine formulations for biological activity using fresh human whole blood.

    Science.gov (United States)

    Brookes, Roger H; Hakimi, Jalil; Ha, Yukyung; Aboutorabian, Sepideh; Ausar, Salvador F; Hasija, Manvi; Smith, Steven G; Todryk, Stephen M; Dockrell, Hazel M; Rahman, Nausheen

    2014-01-01

    Understanding the relevant biological activity of any pharmaceutical formulation destined for human use is crucial. For vaccine-based formulations, activity must reflect the expected immune response, while for non-vaccine therapeutic agents, such as monoclonal antibodies, a lack of immune response to the formulation is desired. During early formulation development, various biochemical and biophysical characteristics can be monitored in a high-throughput screening (HTS) format. However, it remains impractical and arguably unethical to screen samples in this way for immunological functionality in animal models. Furthermore, data for immunological functionality lag formulation design by months, making it cumbersome to relate back to formulations in real-time. It is also likely that animal testing may not accurately reflect the response in humans. For a more effective formulation screen, a human whole blood (hWB) approach can be used to assess immunological functionality. The functional activity relates directly to the human immune response to a complete formulation (adjuvant/antigen) and includes adjuvant response, antigen response, adjuvant-modulated antigen response, stability, and potentially safety. The following commentary discusses the hWB approach as a valuable new tool to de-risk manufacture, formulation design, and clinical progression. PMID:24401565

  5. Data-Driven Derivation of an "Informer Compound Set" for Improved Selection of Active Compounds in High-Throughput Screening.

    Science.gov (United States)

    Paricharak, Shardul; IJzerman, Adriaan P; Jenkins, Jeremy L; Bender, Andreas; Nigsch, Florian

    2016-09-26

    Despite the usefulness of high-throughput screening (HTS) in drug discovery, for some systems, low assay throughput or high screening cost can prohibit the screening of large numbers of compounds. In such cases, iterative cycles of screening involving active learning (AL) are employed, creating the need for smaller "informer sets" that can be routinely screened to build predictive models for selecting compounds from the screening collection for follow-up screens. Here, we present a data-driven derivation of an informer compound set with improved predictivity of active compounds in HTS, and we validate its benefit over randomly selected training sets on 46 PubChem assays comprising at least 300,000 compounds and covering a wide range of assay biology. The informer compound set showed improvement in BEDROC(α = 100), PRAUC, and ROCAUC values averaged over all assays of 0.024, 0.014, and 0.016, respectively, compared to randomly selected training sets, all with paired t-test p-values <10(-15). A per-assay assessment showed that the BEDROC(α = 100), which is of particular relevance for early retrieval of actives, improved for 38 out of 46 assays, increasing the success rate of smaller follow-up screens. Overall, we showed that an informer set derived from historical HTS activity data can be employed for routine small-scale exploratory screening in an assay-agnostic fashion. This approach led to a consistent improvement in hit rates in follow-up screens without compromising scaffold retrieval. The informer set is adjustable in size depending on the number of compounds one intends to screen, as performance gains are realized for sets with more than 3,000 compounds, and this set is therefore applicable to a variety of situations. Finally, our results indicate that random sampling may not adequately cover descriptor space, drawing attention to the importance of the composition of the training set for predicting actives.

  6. Video game genre preference, physical activity and screen-time in adolescent boys from low-income communities.

    Science.gov (United States)

    Thorne, Hayden T; Smith, Jordan J; Morgan, Philip J; Babic, Mark J; Lubans, David R

    2014-12-01

    The primary aim of this study was to examine the association between the types of video games played by adolescent boys and their participation in physical activity and recreational screen-time. Participants were 320 boys (mean age = 12.7, ±0.5 years) from 14 secondary schools located in low-income areas of New South Wales, Australia. Outcomes included height, weight, physical activity (accelerometers), total screen-time, and video game genre preference. Significant differences in both weekday and weekend screen-time were found between video game genre groups. In addition, significant differences in overall activity and moderate-to-vigorous physical activity were found between genre groups on weekdays. Between-group differences in physical activity on weekends were not statistically significant. This cross-sectional study has demonstrated that video game genre preference is associated with physical activity and screen-time in adolescent boys from low-income communities.

  7. Video game genre preference, physical activity and screen-time in adolescent boys from low-income communities.

    Science.gov (United States)

    Thorne, Hayden T; Smith, Jordan J; Morgan, Philip J; Babic, Mark J; Lubans, David R

    2014-12-01

    The primary aim of this study was to examine the association between the types of video games played by adolescent boys and their participation in physical activity and recreational screen-time. Participants were 320 boys (mean age = 12.7, ±0.5 years) from 14 secondary schools located in low-income areas of New South Wales, Australia. Outcomes included height, weight, physical activity (accelerometers), total screen-time, and video game genre preference. Significant differences in both weekday and weekend screen-time were found between video game genre groups. In addition, significant differences in overall activity and moderate-to-vigorous physical activity were found between genre groups on weekdays. Between-group differences in physical activity on weekends were not statistically significant. This cross-sectional study has demonstrated that video game genre preference is associated with physical activity and screen-time in adolescent boys from low-income communities. PMID:25448829

  8. A simple liposome assay for the screening of zinc ionophore activity of polyphenols.

    Science.gov (United States)

    Clergeaud, Gael; Dabbagh-Bazarbachi, Husam; Ortiz, Mayreli; Fernández-Larrea, Juan B; O'Sullivan, Ciara K

    2016-04-15

    An efficient liposomal system for screening the zinc ionophore activity of a selected library consisting of the most relevant dietary polyphenols is presented. The zinc ionophore activity was demonstrated by exploring the use of zinc-specific fluorophore FluoZin-3 loaded liposomes as simple membrane tools that mimic the cell membrane. The zinc ionophore activity was demonstrated as the capacity of polyphenols to transport zinc cations across the liposome membrane and increase the zinc-specific fluorescence of the encapsulated fluorophore FluoZin-3. In addition, the zinc chelation strength of the polyphenols was also tested in a competition assay based on the fluorescence quenching of zinc-dependent fluorescence emitted by zinc-FluoZin-3 complex. Finally, the correlation between the chelation capacity and ionophore activity is demonstrated, thus underlining the sequestering or ionophoric activity that the phenolic compounds can display, thus, providing better knowledge of the importance of the structural conformation versus their biological activity. Furthermore, the assays developed can be used as tools for rapid, high-throughput screening of families of polyphenols towards different biometals. PMID:26617034

  9. A simple liposome assay for the screening of zinc ionophore activity of polyphenols.

    Science.gov (United States)

    Clergeaud, Gael; Dabbagh-Bazarbachi, Husam; Ortiz, Mayreli; Fernández-Larrea, Juan B; O'Sullivan, Ciara K

    2016-04-15

    An efficient liposomal system for screening the zinc ionophore activity of a selected library consisting of the most relevant dietary polyphenols is presented. The zinc ionophore activity was demonstrated by exploring the use of zinc-specific fluorophore FluoZin-3 loaded liposomes as simple membrane tools that mimic the cell membrane. The zinc ionophore activity was demonstrated as the capacity of polyphenols to transport zinc cations across the liposome membrane and increase the zinc-specific fluorescence of the encapsulated fluorophore FluoZin-3. In addition, the zinc chelation strength of the polyphenols was also tested in a competition assay based on the fluorescence quenching of zinc-dependent fluorescence emitted by zinc-FluoZin-3 complex. Finally, the correlation between the chelation capacity and ionophore activity is demonstrated, thus underlining the sequestering or ionophoric activity that the phenolic compounds can display, thus, providing better knowledge of the importance of the structural conformation versus their biological activity. Furthermore, the assays developed can be used as tools for rapid, high-throughput screening of families of polyphenols towards different biometals.

  10. Preliminary phytochemical screening and in vitro antibacterial activity of Anamirta cocculus (Linn. seeds

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    Umer Qadir

    2015-04-01

    Full Text Available The present work is aimed at primary screening of the phytochemical contents of seven solvents (petroleum ether, benzene, chloroform, acetone, methanol, ethanol and a mixture of methanol and ethyl acetate (1:3 extracts of the seeds of Anamirta cocculus (Linn. and to evaluate the antibacterial activity of these extracts against five species of pathogenic bacteria. The powdered seeds of A. cocculus were extracted with seven solvents (polar and non-polar with Soxhlet apparatus and the extracts were subjected to preliminary phytochemical screening by standard biochemical tests. The antibacterial activity of various extracts was evaluated against five bacterial species (Staphylococcus aureus, Proteus vulgaris, Escherichia coli, Salmonella typhi and Klebsiella pneumoniae. The zone of inhibitions and minimum inhibitory concentration (MIC of the various extracts were determined by running the experiments in triplicates. The extracts of the seeds of A. cocculus contained various pharmaceutically active substances viz., aldehydes, alkaloids, phenolic compounds, flavonoids, saponins, carbohydrates, proteins, lipids, glycosides, phytosterols, volatile oils, gums and mucilage and other minor phytochemicals. All the extracts showed significant levels of antibacterial activity. Methanol extract was the most active one with remarkable antibacterial activity on the various species tested. MICs of the extracts revealed methanol extract as the most potent one with the lowest inhibitory concentration of 3 μg/mL on E. coli. The findings of the present study indicated that the seeds of A. cocculus possess various secondary metabolites having the potential for developing pharmaceutical drugs, especially antimicrobial ones.

  11. Anti-infective treatment for the HIV-infected patient during perioperative period%围手术期HIV感染者的抗感染治疗

    Institute of Scientific and Technical Information of China (English)

    刘保池; 张磊; 李垒; 司炎辉; 宋言峥; 赵中辛

    2012-01-01

      Objective:To investigate anti-infective treatments in HIV-infected surgical patients during the perioperative period. Methods 〓 A retrospective study of sepsis and surgical site infections (SSIs) was conducted in 266 HIV-infected patients from January 2009 to December 2011 in Shanghai Public Health Clinical Center. The patients were divided into 3 groups based on CD4 cells counts in the preoperative period: group A (<200 cell/μl), group B (200-349 cell/μl) and group C (≥350 cell/μl). Highly active anti-retrovirus therapy (HAART) was started in group B. Preoperative antibiotic medication SMZ and fluconazole against Pneumocystis carinii pneumonia (PCP) and other fungal infection was started in group A. No special treatment in group C. Results〓There were only 6 patients dead at 30 days after surgery, with the death rate of 2.3%. Sepsis appeared in 110 patients (41.3%). Patients in group A were more likely to get sepsis than patients in the other two groups (P <0.01). Conclusion〓Complete evalua- tion of surgical risk and suitable perioperative anti-infective treatment may lead to better outcome for HIV-infected surgical patients.%  〓〓[]〓目的〓探讨 HIV 感染者围手术期合理的抗感染治疗.方法〓回顾性分析上海市公共卫生临床中心外科2009年1月至2011年12月救治的266例 HIV 感染患者围手术期临床资料,根据患者术前 CD4 T 淋巴细胞水平分 A 组<200 cell/μl,B 组200~349 cell/μl 和 C 组≥350 cell/μl 三组,对 B 组给予抗 HIV 病毒治疗,对 A 组给予抗 HIV 病毒、磺胺甲唑(SMZ)和氟康唑预防肺孢子虫和真菌感染,对已经合并结核、真菌等机会性感染者给予相应的抗感染治疗.对 C组无特殊处理.结果〓经适当的抗感染治疗,266例患者手术后30 d 内死亡6例,病死率2.3%.110例发生脓毒症,脓毒症发生率41.3%.A 组脓毒症发病率明显高于 B 组和 C 组(P <0.01).结论〓精细的手术与合理的围手术

  12. BIOCHEMICAL GENETIC STUDIES ON CUTTLEFISH SEPIELLA MAINDRONI (CEPHALOPODA: SEPIIDAE)- ACTIVE LOCI SCREENING OF ISOZYME

    Institute of Scientific and Technical Information of China (English)

    2001-01-01

    Screening of 46 putative enzyme-coding loci and 4 different kinds of tissues of Sepiella maindroni de Rochebrone, 1884 for enzymatic activities using starch gel electrophoretic technique proved that the 21 enzymes such as AAT, AK, ALP, AP, CK, DIA, ES, FBP, G3PDH, GPI, GRS,IDH, LDH, MDH, MEP, MPI, NP, PGDH, PGM, SOD and XO* , were active to Sepiella maindroni after being stained. The tissue exhibiting stable and clear bands was also determined. Among tissues tested, mantle muscle tissue was the best for electrophoretic survey of isozymes. Buccal bulb muscle, eye and liver were fairly good for some special enzymes, such as DIA, ES, MPI, NP, etc.

  13. Data-Driven Derivation of an "Informer Compound Set" for Improved Selection of Active Compounds in High-Throughput Screening.

    Science.gov (United States)

    Paricharak, Shardul; IJzerman, Adriaan P; Jenkins, Jeremy L; Bender, Andreas; Nigsch, Florian

    2016-09-26

    Despite the usefulness of high-throughput screening (HTS) in drug discovery, for some systems, low assay throughput or high screening cost can prohibit the screening of large numbers of compounds. In such cases, iterative cycles of screening involving active learning (AL) are employed, creating the need for smaller "informer sets" that can be routinely screened to build predictive models for selecting compounds from the screening collection for follow-up screens. Here, we present a data-driven derivation of an informer compound set with improved predictivity of active compounds in HTS, and we validate its benefit over randomly selected training sets on 46 PubChem assays comprising at least 300,000 compounds and covering a wide range of assay biology. The informer compound set showed improvement in BEDROC(α = 100), PRAUC, and ROCAUC values averaged over all assays of 0.024, 0.014, and 0.016, respectively, compared to randomly selected training sets, all with paired t-test p-values screens. Overall, we showed that an informer set derived from historical HTS activity data can be employed for routine small-scale exploratory screening in an assay-agnostic fashion. This approach led to a consistent improvement in hit rates in follow-up screens without compromising scaffold retrieval. The informer set is adjustable in size depending on the number of compounds one intends to screen, as performance gains are realized for sets with more than 3,000 compounds, and this set is therefore applicable to a variety of situations. Finally, our results indicate that random sampling may not adequately cover descriptor space, drawing attention to the importance of the composition of the training set for predicting actives. PMID:27487177

  14. Activity Analysis and Preliminary Inducer Screening of the Chicken DAZL Gene Promoter

    Directory of Open Access Journals (Sweden)

    Lei Zhang

    2015-03-01

    Full Text Available This study was aimed at identifying the active control area of chicken DAZL gene core promoter, to screen optimum inducers of the DAZL gene, thus to enhance the differentiation of embryonic stem cells into spermatogonial stem cells. Fragments of chicken DAZL gene promoter were cloned into fluorescent reporter plasmids and transfected into DF-1 cells. Then Dual-Luciferase® Reporter Assay System was used to identify the activity of the DAZL gene under different inducers. Our studies showed that the DAZL core promoter region for the Suqin yellow chicken was −383 to −39 bp. The dual-luciferase® reporter showed that all-trans retinoic acid (ATRA, a retinoic acid receptor alpha agonist (tamibarotene/Am80, or estradiol (E2 could significantly enhance DAZL transcription. The in vitro inductive culture of chicken ESCs demonstrated that, with ATRA treatment, DAZL transcription peaked at 6 days and then decreased slowly; whereas, DAZL transcription was continuous and peaked at 10 days with Am80 treatment. E2 treatment significantly increased DAZL expression after 8 days. All three treatments were associated with the appearance of male germ cell (MGC-like cells on day 10. These results provide the optimum inducer screening of the DAZL gene and lay the foundation for further screening of compounds that can induce the differentiation of ESCs into MGCs in vitro.

  15. Activity analysis and preliminary inducer screening of the chicken DAZL gene promoter.

    Science.gov (United States)

    Zhang, Lei; Zhu, Rui; Zuo, Qisheng; Li, Dong; Lian, Chao; Tang, Beibei; Xiao, Tianrong; Zhang, Yani; Li, Bichun

    2015-01-01

    This study was aimed at identifying the active control area of chicken DAZL gene core promoter, to screen optimum inducers of the DAZL gene, thus to enhance the differentiation of embryonic stem cells into spermatogonial stem cells. Fragments of chicken DAZL gene promoter were cloned into fluorescent reporter plasmids and transfected into DF-1 cells. Then Dual-Luciferase® Reporter Assay System was used to identify the activity of the DAZL gene under different inducers. Our studies showed that the DAZL core promoter region for the Suqin yellow chicken was -383 to -39 bp. The dual-luciferase® reporter showed that all-trans retinoic acid (ATRA), a retinoic acid receptor alpha agonist (tamibarotene/Am80), or estradiol (E2) could significantly enhance DAZL transcription. The in vitro inductive culture of chicken ESCs demonstrated that, with ATRA treatment, DAZL transcription peaked at 6 days and then decreased slowly; whereas, DAZL transcription was continuous and peaked at 10 days with Am80 treatment. E2 treatment significantly increased DAZL expression after 8 days. All three treatments were associated with the appearance of male germ cell (MGC)-like cells on day 10. These results provide the optimum inducer screening of the DAZL gene and lay the foundation for further screening of compounds that can induce the differentiation of ESCs into MGCs in vitro. PMID:25807265

  16. Tetrandrine identified in a small molecule screen to activate mesenchymal stem cells for enhanced immunomodulation.

    Science.gov (United States)

    Yang, Zijiang; Concannon, John; Ng, Kelvin S; Seyb, Kathleen; Mortensen, Luke J; Ranganath, Sudhir; Gu, Fangqi; Levy, Oren; Tong, Zhixiang; Martyn, Keir; Zhao, Weian; Lin, Charles P; Glicksman, Marcie A; Karp, Jeffrey M

    2016-07-26

    Pre-treatment or priming of mesenchymal stem cells (MSC) prior to transplantation can significantly augment the immunosuppressive effect of MSC-based therapies. In this study, we screened a library of 1402 FDA-approved bioactive compounds to prime MSC. We identified tetrandrine as a potential hit that activates the secretion of prostaglandin E2 (PGE2), a potent immunosuppressive agent, by MSC. Tetrandrine increased MSC PGE2 secretion through the NF-κB/COX-2 signaling pathway. When co-cultured with mouse macrophages (RAW264.7), tetrandrine-primed MSC attenuated the level of TNF-α secreted by RAW264.7. Furthermore, systemic transplantation of primed MSC into a mouse ear skin inflammation model significantly reduced the level of TNF-α in the inflamed ear, compared to unprimed cells. Screening of small molecules to pre-condition cells prior to transplantation represents a promising strategy to boost the therapeutic potential of cell therapy.

  17. Epigenetic Tailoring for the Production of Anti-Infective Cytosporones from the Marine Fungus Leucostoma persoonii

    Directory of Open Access Journals (Sweden)

    Alberto van Olphen

    2012-03-01

    Full Text Available Recent genomic studies have demonstrated that fungi can possess gene clusters encoding for the production of previously unobserved secondary metabolites. Activation of these attenuated or silenced genes to obtain either improved titers of known compounds or new ones altogether has been a subject of considerable interest. In our efforts to discover new chemotypes that are effective against infectious diseases, including malaria and methicillin-resistant Staphylococcus aureus (MRSA, we have isolated a strain of marine fungus, Leucostoma persoonii, that produces bioactive cytosporones. Epigenetic modifiers employed to activate secondary metabolite genes resulted in enhanced production of known cytosporones B (1, 360%, C (2, 580% and E (3, 890%, as well as the production of the previously undescribed cytosporone R (4. Cytosporone E was the most bioactive, displaying an IC90 of 13 µM toward Plasmodium falciparum, with A549 cytotoxicity IC90 of 437 µM, representing a 90% inhibition therapeutic index (TI90 = IC90 A459/IC90 P. falciparum of 33. In addition, cytosporone E was active against MRSA with a minimal inhibitory concentration (MIC of 72 µM and inhibition of MRSA biofilm at roughly half that value (minimum biofilm eradication counts, MBEC90, was found to be 39 µM.

  18. Mussel-inspired alginate gel promoting the osteogenic differentiation of mesenchymal stem cells and anti-infection.

    Science.gov (United States)

    Zhang, Shiwen; Xu, Kaige; Darabi, Mohammad Ali; Yuan, Quan; Xing, Malcolm

    2016-12-01

    Alginate hydrogels have been used in cell encapsulation for many years but a prevalent issue with pure alginates is that they are unable to provide enough bioactive properties to interact with mammalian cells. This paper discusses the modification of alginate with mussel-inspired dopamine for cell loading and anti-infection. Mouse bone marrow stem cells were immobilized into alginate and alginate-dopamine beads and fibers. Through live-dead and MTT assay, alginates modified by dopamine promoted cell viability and proliferation. In vitro cell differentiation results showed that such an alginate-dopamine gel can promote the osteogenic differentiation of mesenchymal stem cell after PCR and ALP assays. In addition to that, the adhesive prosperities of dopamine allowed for coating the surface of alginate-dopamine gel with silver nanoparticles, which provided the gel with significant antibacterial characteristics. Overall, these results demonstrate that a dopamine-modified alginate gel can be a great tool for cell encapsulation to promote cell proliferation and can be applied to bone regeneration, especially in contaminated bone defects. PMID:27612740

  19. Screening SIRT1 Activators from Medicinal Plants as Bioactive Compounds against Oxidative Damage in Mitochondrial Function

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    Yi Wang

    2016-01-01

    Full Text Available Sirtuin type 1 (SIRT1 belongs to the family of NAD+ dependent histone deacetylases and plays a critical role in cellular metabolism and response to oxidative stress. Traditional Chinese medicines (TCMs, as an important part of natural products, have been reported to exert protective effect against oxidative stress in mitochondria. In this study, we screened SIRT1 activators from TCMs and investigated their activities against mitochondrial damage. 19 activators were found in total by in vitro SIRT1 activity assay. Among those active compounds, four compounds, ginsenoside Rb2, ginsenoside F1, ginsenoside Rc, and schisandrin A, were further studied to validate the SIRT1-activation effects by liquid chromatography-mass spectrometry and confirm their activities against oxidative damage in H9c2 cardiomyocytes exposed to tert-butyl hydroperoxide (t-BHP. The results showed that those compounds enhanced the deacetylated activity of SIRT1, increased ATP content, and inhibited intracellular ROS formation as well as regulating the activity of Mn-SOD. These SIRT1 activators also showed moderate protective effects on mitochondrial function in t-BHP cells by recovering oxygen consumption and increasing mitochondrial DNA content. Our results suggested that those compounds from TCMs attenuated oxidative stress-induced mitochondrial damage in cardiomyocytes through activation of SIRT1.

  20. Antimicrobial and host-defense peptides as new anti-infective therapeutic strategies.

    Science.gov (United States)

    Hancock, Robert E W; Sahl, Hans-Georg

    2006-12-01

    Short cationic amphiphilic peptides with antimicrobial and/or immunomodulatory activities are present in virtually every life form, as an important component of (innate) immune defenses. These host-defense peptides provide a template for two separate classes of antimicrobial drugs. Direct-acting antimicrobial host-defense peptides can be rapid-acting and potent, and possess an unusually broad spectrum of activity; consequently, they have prospects as new antibiotics, although clinical trials to date have shown efficacy only as topical agents. But for these compounds to fulfill their therapeutic promise and overcome clinical setbacks, further work is needed to understand their mechanisms of action and reduce the potential for unwanted toxicity, to make them more resistant to protease degradation and improve serum half-life, as well as to devise means of manufacturing them on a large scale in a consistent and cost-effective manner. In contrast, the role of cationic host-defense peptides in modulating the innate immune response and boosting infection-resolving immunity while dampening potentially harmful pro-inflammatory (septic) responses gives these peptides the potential to become an entirely new therapeutic approach against bacterial infections.

  1. Phytochemical screening and In vivo anti-ulcer activity of Ethanolic extract of Heliotropium indicum L

    Directory of Open Access Journals (Sweden)

    S.Nethaji

    2013-12-01

    Full Text Available The phytochemical compounds and anti-ulcer activity of leaves and root extracts of Heliotropium indicum Linn. The preliminary phytochemical screening was performed by in vitromethod and anti-ulcer activity was conducted by in vivomethod. The phytochemical analysis revealed the presence of alkaloids, carbohydrates and glycosides, phytosterols, fixed oils and fats, phenolic compounds and tannins, flavonoids, terpenoids,proteins and amino acids. The ethanolic extract of Heliotropium indicumleaf and root was evaluated for its anti-ulcer activity against pylorous ligation induced gastric ulcer in rats. It was found that significant reduction in gastric volume, free acidity, total acidity and ulcer index. The present study concluded that the H.indicumplant extract have various bioactivecompounds and anti-ulcer activity in animal models against the drug induced gastric ulcer.

  2. Phytochemical screening, antioxidant, and antimicrobial activities of the crude leaves′ extract from Ipomoea batatas (L. Lam

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    Márcia Thaís Pochapski

    2011-01-01

    Full Text Available Background: Ipomoea batatas (L. Lam., popularly known as sweet potato (SP, has played an important role as an energy and a phytochemical source in human nutrition and animal feeding. Ethnopharmacological data show that SP leaves have been effectively used in herbal medicine to treat inflammatory and/or infectious oral diseases in Brazil. The aim of this research was to evaluate the phytochemical, antioxidant, and antimicrobial activities of the crude leaves′ extract of SP leaves. Materials and Methods: The screening was performed for triterpenes/steroids, alkaloids, anthraquinones, coumarins, flavonoids, saponins, tannins, and phenolic acids. The color intensity or the precipitate formation was used as analytical responses to these tests. The total antioxidant capacity was evaluated by the phosphomolybdenum complex method. Antimicrobial activity was made by agar disk and agar well diffusion tests. Results: The phytochemical screening showed positive results for triterpenes/steroids, alkaloids, anthraquinones, coumarins, flavonoids, saponins, tannins, and phenolic acids. Total contents of 345.65, 328.44, and 662.02 mg were respectively obtained for alkaloids, anthraquinones, and phenolic compounds in 100 g of the dry sample. The total antioxidant capacity was 42.94% as compared to ascorbic acid. For antimicrobial studies, no concentration of the SP freeze dried extract was able to inhibit the growth of Streptococcus mutans, S. mitis, Staphylococcus aureus, and Candida albicans in both agar disk and agar well diffusion tests. Conclusions: SP leaves demonstrated the presence of secondary metabolites with potential biological activities. No antimicrobial activity was observed.

  3. ANTIBACTERIAL ACTIVITY AND PHYTOCHEMICAL SCREENING OF LEAVES AND STEM EXTRACTS OF AVICENNIA ALBA BLUME

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    Nagababu, P

    2012-12-01

    Full Text Available The present work was attempted to study the Antibacterial activity and phytochemical analysis of Mangrove plant Avicennia alba. Leaf and stem extracts of A. alba were prepared in Hexane, Benzene, Chloroform, Ethyl acetate, Acetone and Methanol solvents. The resulted extracts of the plant were screened for antibacterial activity against Micrococcus luteus MTCC 106, Arthrobacter protophormiae MTCC 2682, Rhodococcus rhodochrous MTCC 265, Alcaligens faecalis MTCC 126, Proteus- mirabilis MTCC 425, Enterobacter aerogenes MTCC 10208, Proteus vulgaris MTCC 426, Bacillus megaterium MTCC 428, Enterococcus faecalis MTCC 439, Streptococcus mutans- MTCC 497, Salmonella enterica MTCC 3858, Staphylococcus aureus MTCC 737, Pseudomonas aeruginosa MTCC 1688 and Bacillus subtilis MTCC 441. The extracts were also screened for phytochemicals like Carbohydrates, Tannins, Steroids, Terpenoids, Saponins, Flavanoids, Alkaloids and Soluble starch. Of the six solvent extracts of A. alba, ethyl acetate and acetone extracts of leaf and stem, with few exceptions, showed relatively high antibacterial activity. Benzene and chloroform extracts of A. alba showed a larger zone of inhibition against Salmonella enterica than other bacteria. A. alba leaf and stem extracts of different solvents showed good antibacterial activity against Gram negative bacteria than the Gram positive bacteria tested. Most of the solvent extracts of leaf and stem are effective on many bacteria tested than the positive control. The acetone and methanol extracts of leaf and stem showed maximum positive results towards the phytochemical constituents.

  4. Antibiofilm and anti-infection of a marine bacterial exopolysaccharide against Pseudomonas aeruginosa.

    Directory of Open Access Journals (Sweden)

    Shimei eWu

    2016-02-01

    Full Text Available Pseudomonas aeruginosa is a well-known pathogenic bacterium that forms biofilms and produces virulence factors, thus leading to major problems in many fields, such as clinical infection, food contamination and marine biofouling. In this study, we report the purification and characterization of an exopolysaccharide EPS273 from the culture supernatant of marine bacterium Pseudomonas stutzeri 273. The exopolysaccharide EPS273 not only effectively inhibits biofilm formation but also disperses preformed biofilm of Pseudomonas aeruginosa PAO1. High performance liquid chromatography traces of the hydrolyzed polysaccharides shows that EPS273 primarily consists of glucosamine, rhamnose, glucose and mannose. Further investigation demonstrates that EPS273 reduces the production of the virulence factors pyocyanin, exoprotease and rhamnolipid, and the virulence of P. aeruginosa PAO1 to human lung cells A549 and zebrafish embryos is also obviously attenuated by EPS273. In addition, EPS273 also greatly reduces the production of hydrogen peroxide (H2O2 and extracellular DNA (eDNA, which are important factors for biofilm formation. Furthermore, EPS273 exhibits strong antioxidant potential by quenching hydroxyl and superoxide anion radicals. Notably, the antibiofouling activity of EPS273 is observed in the marine environment up to two weeks according to the amounts of bacteria and diatoms in the glass slides submerged in the ocean. Taken together, the properties of EPS273 indicate that it has a promising prospect in combating bacterial biofilm-associated infection, food-processing contamination and marine biofouling.

  5. Antibiofilm and Anti-Infection of a Marine Bacterial Exopolysaccharide Against Pseudomonas aeruginosa.

    Science.gov (United States)

    Wu, Shimei; Liu, Ge; Jin, Weihua; Xiu, Pengyuan; Sun, Chaomin

    2016-01-01

    Pseudomonas aeruginosa is a well-known pathogenic bacterium that forms biofilms and produces virulence factors, thus leading to major problems in many fields, such as clinical infection, food contamination, and marine biofouling. In this study, we report the purification and characterization of an exopolysaccharide EPS273 from the culture supernatant of marine bacterium P. stutzeri 273. The exopolysaccharide EPS273 not only effectively inhibits biofilm formation but also disperses preformed biofilm of P. aeruginosa PAO1. High performance liquid chromatography traces of the hydrolyzed polysaccharides shows that EPS273 primarily consists of glucosamine, rhamnose, glucose and mannose. Further investigation demonstrates that EPS273 reduces the production of the virulence factors pyocyanin, exoprotease, and rhamnolipid, and the virulence of P. aeruginosa PAO1 to human lung cells A549 and zebrafish embryos is also obviously attenuated by EPS273. In addition, EPS273 also greatly reduces the production of hydrogen peroxide (H2O2) and extracellular DNA (eDNA), which are important factors for biofilm formation. Furthermore, EPS273 exhibits strong antioxidant potential by quenching hydroxyl and superoxide anion radicals. Notably, the antibiofouling activity of EPS273 is observed in the marine environment up to 2 weeks according to the amounts of bacteria and diatoms in the glass slides submerged in the ocean. Taken together, the properties of EPS273 indicate that it has a promising prospect in combating bacterial biofilm-associated infection, food-processing contamination and marine biofouling. PMID:26903981

  6. Anti-infective efficacy of the lactoferrin-derived antimicrobial peptide HLR1r.

    Science.gov (United States)

    Björn, Camilla; Mahlapuu, Margit; Mattsby-Baltzer, Inger; Håkansson, Joakim

    2016-07-01

    Antimicrobial peptides (AMPs) have emerged as a new class of drug candidates for the treatment of infectious diseases. Here we describe a novel AMP, HLR1r, which is structurally derived from the human milk protein lactoferrin and demonstrates a broad spectrum microbicidal action in vitro. The minimum concentration of HLR1r needed for killing ≥99% of microorganisms in vitro, was in the range of 3-50μg/ml for common Gram-negative and Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA), and for the yeast Candida albicans, when assessed in diluted brain-heart infusion medium. We found that HLR1r also possesses anti-inflammatory properties as evidenced by inhibition of tumor necrosis factor alpha (TNF-α) secretion from human monocyte-derived macrophages and by repression of interleukin-6 (IL-6) and plasminogen activator inhibitor-1 (PAI-1) secretion from human mesothelial cells, without any cytotoxic effect observed at the concentration range tested (up to 400μg/ml). HLR1r demonstrated pronounced anti-infectious effect in in vivo experimental models of cutaneous candidiasis in mice and of excision wounds infected with MRSA in rats as well as in an ex vivo model of pig skin infected with S. aureus. In conclusion, HLR1r may constitute a new therapeutic alternative for local treatment of skin infections. PMID:27155369

  7. INFECTIOUS AETIOLOGY OF MARGINAL ZONE LYMPHOMA AND ROLE OF ANTI-INFECTIVE THERAPY

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    Salvatore Perrone

    2016-01-01

    Full Text Available Marginal zone lymphomas have been associated with several infectious agents covering both viral and bacterial pathogens and in some cases a clear aetiological role has been established. Pathogenetic mechanisms are currently not completely understood, however the role of chronic stimulation of the host immune response with persistent lymphocyte activation represents the most convincing explanation for lymphoproliferation. Gastric MALT lymphoma is strictly associated with Helicobacter pylori infection and various eradicating protocols, developed due to increasing antibiotic resistance, represent the first line therapy. The response rate to eradication is good with 80% of response at 1 year; this finding is also noteworthy because recapitulates a cancer cured only by antibacterial approach and it satisfies the Koch postulates of causation, establishing a causative relationship between Hp and gastric MALT lymphoma. Patients with chronic HCV infection have 5 times higher risk to develop MZL, in particular an association with splenic and nodal MZL has been shown in several studies. Moreover, there is evidence of lymphoma regression after antiviral therapy with interferon+ribavirin, thus rising hope that new available drugs, extremely effective against HCV replication, could improve outcome also in HCV-driven lymphomas. The rare cases of MZL localized to orbital fat and eye conjunctivas have been associated with Chlamydia psittaci infection carried by birds. Efficacy of antibacterial therapy against C. psittaci are conflicting and generally poorer thain gastric MALT. Finally some case-reports will cover the relationship between primary cutaneous B-cell Lymphomas and Borrelia Burgdorferi.

  8. An anti-infective peptide that selectively modulates the innate immune response.

    Science.gov (United States)

    Scott, Monisha G; Dullaghan, Edie; Mookherjee, Neeloffer; Glavas, Natalie; Waldbrook, Matthew; Thompson, Annick; Wang, Aikun; Lee, Ken; Doria, Silvana; Hamill, Pam; Yu, Jie Jessie; Li, Yuexin; Donini, Oreola; Guarna, M Marta; Finlay, B Brett; North, John R; Hancock, Robert E W

    2007-04-01

    We show that an innate defense-regulator peptide (IDR-1) was protective in mouse models of infection with important Gram-positive and Gram-negative pathogens, including methicillin-resistant Staphylococcus aureus, vancomycin-resistant Enterococcus and Salmonella enterica serovar Typhimurium. When given from 48 h before to 6 h after infection, the peptide was effective by both local and systemic administration. Because protection by IDR-1 was prevented by in vivo depletion of monocytes and macrophages, but not neutrophils or B- and T-lymphocytes, we conclude that monocytes and macrophages are key effector cells. IDR-1 was not directly antimicrobial: gene and protein expression analysis in human and mouse monocytes and macrophages indicated that IDR-1, acting through mitogen-activated protein kinase and other signaling pathways, enhanced the levels of monocyte chemokines while reducing pro-inflammatory cytokine responses. To our knowledge, an innate defense regulator that counters infection by selective modulation of innate immunity without obvious toxicities has not been reported previously.

  9. The Quest for Anti-inflammatory and Anti-infective Biomaterials in Clinical Translation.

    Science.gov (United States)

    Griffith, May; Islam, Mohammad M; Edin, Joel; Papapavlou, Georgia; Buznyk, Oleksiy; Patra, Hirak K

    2016-01-01

    Biomaterials are now being used or evaluated clinically as implants to supplement the severe shortage of available human donor organs. To date, however, such implants have mainly been developed as scaffolds to promote the regeneration of failing organs due to old age or congenital malformations. In the real world, however, infection or immunological issues often compromise patients. For example, bacterial and viral infections can result in uncontrolled immunopathological damage and lead to organ failure. Hence, there is a need for biomaterials and implants that not only promote regeneration but also address issues that are specific to compromised patients, such as infection and inflammation. Different strategies are needed to address the regeneration of organs that have been damaged by infection or inflammation for successful clinical translation. Therefore, the real quest is for multifunctional biomaterials with combined properties that can combat infections, modulate inflammation, and promote regeneration at the same time. These strategies will necessitate the inclusion of methodologies for management of the cellular and signaling components elicited within the local microenvironment. In the development of such biomaterials, strategies range from the inclusion of materials that have intrinsic anti-inflammatory properties, such as the synthetic lipid polymer, 2-methacryloyloxyethyl phosphorylcholine (MPC), to silver nanoparticles that have antibacterial properties, to inclusion of nano- and micro-particles in biomaterials composites that deliver active drugs. In this present review, we present examples of both kinds of materials in each group along with their pros and cons. Thus, as a promising next generation strategy to aid or replace tissue/organ transplantation, an integrated smart programmable platform is needed for regenerative medicine applications to create and/or restore normal function at the cell and tissue levels. Therefore, now it is of utmost

  10. The Quest for Anti-inflammatory and Anti-infective Biomaterials in Clinical Translation

    Science.gov (United States)

    Griffith, May; Islam, Mohammad M.; Edin, Joel; Papapavlou, Georgia; Buznyk, Oleksiy; Patra, Hirak K.

    2016-01-01

    Biomaterials are now being used or evaluated clinically as implants to supplement the severe shortage of available human donor organs. To date, however, such implants have mainly been developed as scaffolds to promote the regeneration of failing organs due to old age or congenital malformations. In the real world, however, infection or immunological issues often compromise patients. For example, bacterial and viral infections can result in uncontrolled immunopathological damage and lead to organ failure. Hence, there is a need for biomaterials and implants that not only promote regeneration but also address issues that are specific to compromised patients, such as infection and inflammation. Different strategies are needed to address the regeneration of organs that have been damaged by infection or inflammation for successful clinical translation. Therefore, the real quest is for multifunctional biomaterials with combined properties that can combat infections, modulate inflammation, and promote regeneration at the same time. These strategies will necessitate the inclusion of methodologies for management of the cellular and signaling components elicited within the local microenvironment. In the development of such biomaterials, strategies range from the inclusion of materials that have intrinsic anti-inflammatory properties, such as the synthetic lipid polymer, 2-methacryloyloxyethyl phosphorylcholine (MPC), to silver nanoparticles that have antibacterial properties, to inclusion of nano- and micro-particles in biomaterials composites that deliver active drugs. In this present review, we present examples of both kinds of materials in each group along with their pros and cons. Thus, as a promising next generation strategy to aid or replace tissue/organ transplantation, an integrated smart programmable platform is needed for regenerative medicine applications to create and/or restore normal function at the cell and tissue levels. Therefore, now it is of utmost

  11. Screen printed barium titanate thick films prepared from mechanically activated powders

    Energy Technology Data Exchange (ETDEWEB)

    Stojanovic, B.D. [Universidad Estadual Paulista, Sao Paulo (Brazil). Inst. de Quimica; Belgrade Univ. (Yugoslavia). Center for Multidisciplinary Studies; Foschini, C.R.; Varela, J.A. [Universidad Estadual Paulista, Sao Paulo (Brazil). Inst. de Quimica; Pejovic, V.Z. [IRITEL, Belgrade (Yugoslavia); Pavlovic, V.B. [Faculty for Agriculture, Dept. of Physics, UB (Yugoslavia); Pavlovic, V.P. [Faculty for Mechanical Engineering, Dept. of Physics, UB (Yugoslavia)

    2002-07-01

    Barium titanate thick films were prepared from mechanically activated powders based on BaCO{sub 3} and TiO{sub 2}. The thick films were screen-printed on alumina substrates electroded with Ag/Pd. The BT films were sintered at 850 C for 1 hour. The thickness was 30-75 {mu}m depending of number of layers. The microstructure of thick films and the compatibility between BT layers and substrate was investigated by SEM. The dielectric properties were measured and the results were reported. (orig.)

  12. Screening of cytotoxic activity in hexanic and ethanolic extracts of Rollinia laurifolia

    OpenAIRE

    Cunha, M.M.; F.C. NASCIMENTO; Santos Pimento, L. P.; M.A.D. Boaventura; C.E. Salas; M. T. P. Lopes

    2009-01-01

    The hexanic and ethanolic extracts obtained from Rollinia laurifolia, collected in Minas Gerais State/Brazil, were screened by the brine shrimp lethality and cytotoxic assays on different cell lines, in order to identify potential sources for novel antitumoral compounds. Fifty percent of the ethanolic derived fractions (E) showed significant cytotoxic activity (IC50 < 10–1 μg/mL), not related to tannins or saponins, i. e., IC50 E13 on C6 = 1.54 x 10-2 μg/mL, IC50 E29 on L9...

  13. A Sleeping Beauty screen reveals NF-kB activation in CLL mouse model

    Science.gov (United States)

    Zanesi, Nicola; Balatti, Veronica; Riordan, Jesse; Burch, Aaron; Rizzotto, Lara; Palamarchuk, Alexey; Cascione, Luciano; Lagana, Alessandro; Dupuy, Adam J.; Croce, Carlo M.

    2013-01-01

    TCL1 oncogene is overexpressed in aggressive form of human chronic lymphocytic leukemia (CLL) and its dysregulation in mouse B cells causes a CD5-positive leukemia similar to the aggressive form of human CLLs. To identify oncogenes that cooperate with Tcl1, we performed genetic screen in Eμ−TCL1 mice using Sleeping Beauty transposon-mediated mutagenesis. Analysis of transposon common insertion sites identified 7 genes activated by transposon insertions. Overexpression of these genes in mouse CLL was confirmed by real time reverse transcription-polymerase chain reaction. Interestingly, the main known function of 4 of 7 genes (Nfkb1, Tab2, Map3K14, and Nfkbid) is participation in or activation of the nuclear factor-kB (NF-kB) pathway. In addition, activation of the NF-kB is 1 of main functions of Akt2, also identified in the screen. These findings demonstrate cooperation of Tcl1 and the NF-kB pathway in the pathogenesis of aggressive CLL. Identification cooperating cancer genes will result in the development of combinatorial therapies to treat CLL. PMID:23591791

  14. Contact-based ligand-clustering approach for the identification of active compounds in virtual screening

    Directory of Open Access Journals (Sweden)

    Mantsyzov AB

    2012-09-01

    Full Text Available Alexey B Mantsyzov,1 Guillaume Bouvier,2 Nathalie Evrard-Todeschi,1 Gildas Bertho11Université Paris Descartes, Sorbonne, Paris, France; 2Institut Pasteur, Paris, FranceAbstract: Evaluation of docking results is one of the most important problems for virtual screening and in silico drug design. Modern approaches for the identification of active compounds in a large data set of docked molecules use energy scoring functions. One of the general and most significant limitations of these methods relates to inaccurate binding energy estimation, which results in false scoring of docked compounds. Automatic analysis of poses using self-organizing maps (AuPosSOM represents an alternative approach for the evaluation of docking results based on the clustering of compounds by the similarity of their contacts with the receptor. A scoring function was developed for the identification of the active compounds in the AuPosSOM clustered dataset. In addition, the AuPosSOM efficiency for the clustering of compounds and the identification of key contacts considered as important for its activity, were also improved. Benchmark tests for several targets revealed that together with the developed scoring function, AuPosSOM represents a good alternative to the energy-based scoring functions for the evaluation of docking results.Keywords: scoring, docking, virtual screening, CAR, AuPosSOM

  15. Anti-Infective Metabolites of a Newly Isolated Bacillus thuringiensis KL1 Associated with Kalmegh (Andrographis paniculata Nees.), a Traditional Medicinal Herb

    OpenAIRE

    Sudipta Roy; Sahana Yasmin; Subhadeep Ghosh; Somesankar Bhattacharya; Debdulal Banerjee

    2016-01-01

    This study was conducted to isolate endophytic bacteria possessing anti-infective property from Kalmegh (Andrographis paniculata Nees.), a well-known medicinal plant. A total of 23 strains were isolated from this plant among which the strain KL1, isolated from surface-sterilized leaf of this medicinal herb, showed broad-spectrum antagonism against an array of Gram-positive and -negative bacterial pathogens. Ethyl acetate extract of KL1-fermented media yielded a greenish amorphous substance re...

  16. Activity-guided screening of the antioxidants from Paulownia tomentosa var. tomentosa Bark

    Directory of Open Access Journals (Sweden)

    Chuan-Ling Si

    2013-02-01

    Full Text Available Tree barks, as a type of forestry residues, are a rich and renewable bioresource that can produce high value-added products. Paulownia tomentosa var. tomentosa (PTT has been extensively used in traditional Chinese medicine to cure various diseases. However, the antioxidative activity of the chemical constituents of the tree has not yet been investigated. In this study, the bark of PTT were extracted and fractioned. Then the resulting ethyl acetate (EtOAc soluble fraction, which exhibited the strongest antioxidative effect, was subjected to repeated open column chromatography for purification. The screening process was carried out under the guidance antioxidative activity via diphenylpicrylhydrazyl (DPPH radical scavenging assay. Eight phenolic compounds, glucodistylin (I, luteolin (II, ellagic acid (III, cistanoside F (IV, campneoside II (V, isocampneoside II (VI, verbascoside (VII, and isoverbascoside (VIII, were isolated and their structures were elucidated by various spectroscopic analyses. Among the phenolics, II~VIII showed significant antioxidative activity.

  17. Screening of medicinal natural extracts for their antibacterial activity against salmonella species

    International Nuclear Information System (INIS)

    The present study was aimed to screen out natural crude extracts exhibiting antibacterial activity against Salmonella causing gastrointestinal problems in humans. Fifteen Salmonella species were isolated from uncooked chicken, polluted water, rotten potatoes, beef, rotten eggs etc. Aqueous plant extracts of Allium sativum (garlic), Nigella sativa (kalvanji), Azadirachta indica (neem), Ficus carica (anjeer), and Trigonella foenum-graecum (methi) were checked against Salmonella species by well plate method. In addition to plant extract, Honey was also used for antibacterial activity. Inhibition zones ranging from 2mm to 20mm were obtained with different concentration of plant extracts and honey. The antibacterial sensitivity pattern was in the order of kalvanji > garlic > honey > anjeer > methi > neem. The standard antibiotics such as Ceftriaxone and Ciprofloxacin were also used for comparison with natural extract for antibacterial activity. The extracts of Allium sativum, Nigella sativa and Honey were found to be more effective against Salmonella species for which even Ceftriaxone was found ineffective. (author)

  18. Molecular screening of Chinese medicinal plants for progestogenic and anti-progestogenic activity

    Indian Academy of Sciences (India)

    H M Manir Ahmed; Jan-Ying Yeh; Yi-Chia Tang; Winston Teng-Kuei Cheng; Bor-Rung Ou

    2014-06-01

    Estrogen and progestins have adverse effects, and many of these adverse effects are caused by progestins. Due to this, many women choose to use botanical alternatives for hormone replacement therapy, which does not trigger steroidogenic properties. Therefore, it is necessary to screen these herbs for progestogenic and anti-progestogenic properties. Extract of 13 Chinese medicinal plants were analysed for progestogenic and anti-progestogenic activities by using progesterone response element-driven luciferase reporter gene bioassay. MTT assay was carried out to investigate the cytotoxic effect of herb extract on PAE cells. Among the 13 herbs, Dipsacus asperoides extract exhibited progestogenic activity, and 10 species – Cortex eucommiae, Folium artemisiae argyi, Glycyrrhiza uralensis, Angelica sinensis, Atractylodes macrocephala koidz, Scutellaria baicalensis, Cuscuta chinensis, Euscaphis japonica, Ailanthus altissima, and Dioscorea opposita – were recognized to have anti-progestogenic like activities. Extract of Dipsacus asperoides demonstrated dose-dependent progestogenic activity, and the progestogenic activity of 100 g/mL extracts was equivalent to 31.45 ng/mL progesterone activity. Herbs extracts that exhibited anti-progestogenic-like activity also inhibited the 314.46 ng/mL progesterone activity in a dose-response manner. None of the herb extracts shown significant toxic effect on PAE cells at 40–100 g/mL compared to control. This discovery will aid selection of suitable herbs for hormone replacement therapy.

  19. Gametocytocidal screen identifies novel chemical classes with Plasmodium falciparum transmission blocking activity.

    Directory of Open Access Journals (Sweden)

    Natalie G Sanders

    Full Text Available Discovery of transmission blocking compounds is an important intervention strategy necessary to eliminate and eradicate malaria. To date only a small number of drugs that inhibit gametocyte development and thereby transmission from the mosquito to the human host exist. This limitation is largely due to a lack of screening assays easily adaptable to high throughput because of multiple incubation steps or the requirement for high gametocytemia. Here we report the discovery of new compounds with gametocytocidal activity using a simple and robust SYBR Green I- based DNA assay. Our assay utilizes the exflagellation step in male gametocytes and a background suppressor, which masks the staining of dead cells to achieve healthy signal to noise ratio by increasing signal of viable parasites and subtracting signal from dead parasites. By determining the contribution of exflagellation to fluorescent signal and using appropriate cutoff values, we were able to screen for gametocytocidal compounds. After assay validation and optimization, we screened an FDA approved drug library of approximately 1500 compounds, as well as the 400 compound MMV malaria box and identified 44 gametocytocidal compounds with sub to low micromolar IC50s. Major classes of compounds with gametocytocidal activity included quaternary ammonium compounds with structural similarity to choline, acridine-like compounds similar to quinacrine and pyronaridine, as well as antidepressant, antineoplastic, and anthelminthic compounds. Top drug candidates showed near complete transmission blocking in membrane feeding assays. This assay is simple, reproducible and demonstrated robust Z-factor values at low gametocytemia levels, making it amenable to HTS for identification of novel and potent gametocytocidal compounds.

  20. Screening of xylanase activity of Streptomyces albidoflavus PSM-3n isolated from Uttarakhand

    Directory of Open Access Journals (Sweden)

    Pushpendra Sharma

    2013-07-01

    Full Text Available Background: Awareness towards the environmental pollution had made the evolution of green technology by which enzymes got special attention in industries. The enzymes replaced chemical catalysts in manufacturing various chemicals, agricultural and pharmaceutical products. Material and methods: Actinomycetes were isolated and screened for their ability to produce xylanase. For the most promising isolate, selection of media, effect of pH, temperature, metal ions, and detergents on enzyme production and activity was studied. Results: Out of 29 isolates, 22 isolates showed xylanase activity. Out of 22 xylanase producing isolate, 05 isolates were selected for secondary screening on the basis of their clear zone size. The most promising isolate PSM-3n was identified as Streptomyces albidoflavus. It produces maximum enzyme (xylanase in media Horikoshi and Ikura having carbon and nitrogen sources as oat meal and urea respectively. The optimum pH and temperature for the enzyme production was 4.0 and 45°C respectively. The enzyme activity was found maximum at temperature 50°C and enhanced in the presence of Fe3+ ions. There was a reduction in the enzyme activity in the presence of detergents like SDS, tween-20 and tween-80. The enzyme was fairly stable at 50°C for 1 h. Conclusion: The enzyme produced by the isolate PSM-3n is fairly heat stable and highly acid stable. The activity of the enzyme was increased in presence of Fe3+ ions while decreased in presence of SDS. Therefore, further studies are required for purification of xylanase for its application potential in pulp bioleaching processes and in the functional food industry.

  1. A Global Genomic Screening Strategy Reveals Diverse Activators of Constitutive Activated Receptor (CAR)

    Science.gov (United States)

    A comprehensive survey of conditions that activate CAR in the mouse liver has not been carried out but would be useful in understanding their impact on CAR-dependent liver tumor induction. A gene signature dependent on CAR activation was identified by comparing the transcript pr...

  2. In vitro antimicrobial activity and phytochemical screening of clematis species indigenous to Ethiopia

    Directory of Open Access Journals (Sweden)

    S Hawaze

    2012-01-01

    Full Text Available The leaves extracts of two indigenous plants of Ethiopia: Clematis longicauda steud ex A. Rich. and Clematis burgensis Engl. are used in Southwestern Ethiopia to treat otorrhoea and eczema. Antimicrobial activity and MIC of crude extracts were determined by disk diffusion and broth dilution. Phytochemical screening was performed on the extracts. The methanol and petroleum ether extracts of both plants showed antibacterial and antifungal activity. Sensitivity of reference strains was concentration dependent. Methanol and petroleum ether extracts of C. burgensis leaves exerted greater inhibitory effects than C. longicauda extracts whereas aqueous extracts of both plants were inactive. The MIC study revealed a concentration of 0.78 mg/ml on bacteria and 3.125 mg/ml on fungi for methanol extract and 1.56 mg/ml on both fungi and bacteria for petroleum ether extract. Phytochemical screening results indicated the presence of proteins, fixed oils, carbohydrates, tannins, saponins, flavonoids, and steroids. Preliminary chromatographic investigation showed fluorescing spots with R f values that ranged from 0.05 to 0.96 for phenolic compounds and saponins. As the study is one of the first reports on the two indigenous species of Clematis; isolation, purification and characterization of the different primary and secondary metabolites may further yield alternative options to the microbial chemotherapy.

  3. Proposal for a screening test to evaluate the fate of organic micropollutants in activated sludge.

    Science.gov (United States)

    Salvetti, Roberta; Vismara, Renato; Dal Ben, Ilaria; Gorla, Elena; Romele, Laura

    2011-04-01

    The concentrations of organic micropollutants are usually low in wastewaters (order of magnitude of mg L(-1)). However, their emission standards, especially in the case of carcinogenic and bioaccumulating substances, are often much lower (order of magnitude of microg L(-1)). Since these substances, in some cases, can be adsorbable or volatile, their removal via volatilization, biodegradation or sludge adsorption in a wastewater treatment plant (WWTP) becomes a significant feature to include in the usual design process, in order to verify the emission standards in gas and sludge too. In this study a simple screening batch test for the evaluation of the fate of organic micropollutants in water, air and sludge is presented. The test is set up by means of simple laboratory instruments and simulates an activated sludge tank process. In this study the results obtained for four substances with different chemical properties (i.e. toluene, benz(a)anthracene, phenol and benzene) are presented. The screening test proposed can be a useful tool to assess in about one month the fate of organic micropollutants in an activated sludge tank of a WWTP. Moreover, the test can constitute a useful support in the use of mathematical models, since it allows the verification of model results and the calibration of the reactions involved in the removal process. PMID:21877546

  4. Phytochemical Screening, Proximate Analysis and Antioxidant Activity of Dracaena reflexa Lam. Leaves.

    Science.gov (United States)

    Shukla, Abha; Vats, Swati; Shukla, R K

    2015-01-01

    In the present study, the antioxidant activity of successive leaf extracts of Dracaena reflexa was investigated using the scavenging activity on 1,1-diphenyl-2-picrylhydrazyl and reducing power by ferric reducing antioxidant power assay. Methanol extract was found potent in both the assays. IC50 values of 1,1-diphenyl-2-picrylhydrazyl assay for methanol extract was 0.97 mg/ml and ferric reducing antioxidant power value for the same is 1.19. Phytochemical screening, proximate analysis and total phenolic content were also determined. Qualitative screening for phytochemical showed the presence of alkaloids, flavonoids, terpenoids, glycosides and saponins. Highest phenolic content was shown by methanol extract (49.69 mg gallic acid equivalent/g dry weight). Proximate analysis showed moisture content (3.31%), ash content (8.02%), crude fibre (1.31%), crude fat (0.97%), total protein (3.70%), total carbohydrate (86.01) and nutritive value (367.56 kcal/100 g), which would make it a potential nutraceutical. This study suggested that Dracaena reflexa, a potential natural free radical scavenger, which could find use as an antioxidative.

  5. Phytochemical Screening, proximate analysis and antioxidant activity of Dracaena reflexa lam. leaves

    Directory of Open Access Journals (Sweden)

    Abha Shukla

    2015-01-01

    Full Text Available In the present study, the antioxidant activity of successive leaf extracts of Dracaena reflexa was investigated using the scavenging activity on 1,1-diphenyl-2-picrylhydrazyl and reducing power by ferric reducing antioxidant power assay. Methanol extract was found potent in both the assays. IC50 values of 1,1-diphenyl-2-picrylhydrazyl assay for methanol extract was 0.97 mg/ml and ferric reducing antioxidant power value for the same is 1.19. Phytochemical screening, proximate analysis and total phenolic content were also determined. Qualitative screening for phytochemical showed the presence of alkaloids, flavonoids, terpenoids, glycosides and saponins. Highest phenolic content was shown by methanol extract (49.69 mg gallic acid equivalent/g dry weight. Proximate analysis showed moisture content (3.31%, ash content (8.02%, crude fibre (1.31%, crude fat (0.97%, total protein (3.70%, total carbohydrate (86.01 and nutritive value (367.56 kcal/100 g, which would make it a potential nutraceutical. This study suggested that Dracaena reflexa, a potential natural free radical scavenger, which could find use as an antioxidative.

  6. Phytochemical Screening, Proximate Analysis and Antioxidant Activity of Dracaena reflexa Lam. Leaves.

    Science.gov (United States)

    Shukla, Abha; Vats, Swati; Shukla, R K

    2015-01-01

    In the present study, the antioxidant activity of successive leaf extracts of Dracaena reflexa was investigated using the scavenging activity on 1,1-diphenyl-2-picrylhydrazyl and reducing power by ferric reducing antioxidant power assay. Methanol extract was found potent in both the assays. IC50 values of 1,1-diphenyl-2-picrylhydrazyl assay for methanol extract was 0.97 mg/ml and ferric reducing antioxidant power value for the same is 1.19. Phytochemical screening, proximate analysis and total phenolic content were also determined. Qualitative screening for phytochemical showed the presence of alkaloids, flavonoids, terpenoids, glycosides and saponins. Highest phenolic content was shown by methanol extract (49.69 mg gallic acid equivalent/g dry weight). Proximate analysis showed moisture content (3.31%), ash content (8.02%), crude fibre (1.31%), crude fat (0.97%), total protein (3.70%), total carbohydrate (86.01) and nutritive value (367.56 kcal/100 g), which would make it a potential nutraceutical. This study suggested that Dracaena reflexa, a potential natural free radical scavenger, which could find use as an antioxidative. PMID:26798184

  7. In vitro Antimicrobial Activity and Phytochemical Screening of Clematis Species Indigenous to Ethiopia.

    Science.gov (United States)

    Hawaze, S; Deti, H; Suleman, S

    2012-01-01

    THE LEAVES EXTRACTS OF TWO INDIGENOUS PLANTS OF ETHIOPIA: Clematis longicauda steud ex A. Rich. and Clematis burgensis Engl. are used in Southwestern Ethiopia to treat otorrhoea and eczema. Antimicrobial activity and MIC of crude extracts were determined by disk diffusion and broth dilution. Phytochemical screening was performed on the extracts. The methanol and petroleum ether extracts of both plants showed antibacterial and antifungal activity. Sensitivity of reference strains was concentration dependent. Methanol and petroleum ether extracts of C. burgensis leaves exerted greater inhibitory effects than C. longicauda extracts whereas aqueous extracts of both plants were inactive. The MIC study revealed a concentration of 0.78 mg/ml on bacteria and 3.125 mg/ml on fungi for methanol extract and 1.56 mg/ml on both fungi and bacteria for petroleum ether extract. Phytochemical screening results indicated the presence of proteins, fixed oils, carbohydrates, tannins, saponins, flavonoids, and steroids. Preliminary chromatographic investigation showed fluorescing spots with R(f) values that ranged from 0.05 to 0.96 for phenolic compounds and saponins. As the study is one of the first reports on the two indigenous species of Clematis; isolation, purification and characterization of the different primary and secondary metabolites may further yield alternative options to the microbial chemotherapy. PMID:23204619

  8. Daily physical activity and screen time, but not other sedentary activities, are associated with measures of obesity during childhood.

    Science.gov (United States)

    Lee, Shoo Thien; Wong, Jyh Eiin; Shanita, Safii Nik; Ismail, Mohd Noor; Deurenberg, Paul; Poh, Bee Koon

    2015-01-01

    Childhood obesity is related to low physical activity level and a sedentary lifestyle. The aim of this study was to assess the physical activity level and sedentary behaviour of Malaysian children aged 7 to 12 years and to examine their association with body mass index (BMI), BMI-for-age Z-score (BAZ), body fatness (%BF) and waist circumference (WC). A total of 1736 children, representing all ethnic groups were recruited from six regions of Malaysia. Anthropometric measurements included body weight, height and waist circumference. Body fat percentage (%BF) was assessed using bioelectrical impedance. Physical activity was assessed by a physical activity questionnaire (PAQ) in all children and by pedometers in a subsample (n = 514). PAQ score and pedometer step counts were negatively associated with BMI, BAZ, %BF and WC after adjusting for covariates. Screen time was positively associated with BAZ and WC. However, other sedentary activities were not significantly related with any anthropometric indicators. Strategies to promote active living among children in Malaysia should focus not only on increasing physical activity but also emphasise reduction in sedentary behaviours. PMID:25546277

  9. Daily Physical Activity and Screen Time, but Not Other Sedentary Activities, Are Associated with Measures of Obesity during Childhood

    Directory of Open Access Journals (Sweden)

    Shoo Thien Lee

    2014-12-01

    Full Text Available Childhood obesity is related to low physical activity level and a sedentary lifestyle. The aim of this study was to assess the physical activity level and sedentary behaviour of Malaysian children aged 7 to 12 years and to examine their association with body mass index (BMI, BMI-for-age Z-score (BAZ, body fatness (%BF and waist circumference (WC. A total of 1736 children, representing all ethnic groups were recruited from six regions of Malaysia. Anthropometric measurements included body weight, height and waist circumference. Body fat percentage (%BF was assessed using bioelectrical impedance. Physical activity was assessed by a physical activity questionnaire (PAQ in all children and by pedometers in a subsample (n = 514. PAQ score and pedometer step counts were negatively associated with BMI, BAZ, %BF and WC after adjusting for covariates. Screen time was positively associated with BAZ and WC. However, other sedentary activities were not significantly related with any anthropometric indicators. Strategies to promote active living among children in Malaysia should focus not only on increasing physical activity but also emphasise reduction in sedentary behaviours.

  10. Daily physical activity and screen time, but not other sedentary activities, are associated with measures of obesity during childhood.

    Science.gov (United States)

    Lee, Shoo Thien; Wong, Jyh Eiin; Shanita, Safii Nik; Ismail, Mohd Noor; Deurenberg, Paul; Poh, Bee Koon

    2015-01-01

    Childhood obesity is related to low physical activity level and a sedentary lifestyle. The aim of this study was to assess the physical activity level and sedentary behaviour of Malaysian children aged 7 to 12 years and to examine their association with body mass index (BMI), BMI-for-age Z-score (BAZ), body fatness (%BF) and waist circumference (WC). A total of 1736 children, representing all ethnic groups were recruited from six regions of Malaysia. Anthropometric measurements included body weight, height and waist circumference. Body fat percentage (%BF) was assessed using bioelectrical impedance. Physical activity was assessed by a physical activity questionnaire (PAQ) in all children and by pedometers in a subsample (n = 514). PAQ score and pedometer step counts were negatively associated with BMI, BAZ, %BF and WC after adjusting for covariates. Screen time was positively associated with BAZ and WC. However, other sedentary activities were not significantly related with any anthropometric indicators. Strategies to promote active living among children in Malaysia should focus not only on increasing physical activity but also emphasise reduction in sedentary behaviours.

  11. Population-based cohort study of anti-infective medication use before and after the onset of type 1 diabetes in children and adolescents.

    Science.gov (United States)

    Fazeli Farsani, Soulmaz; Souverein, Patrick C; van der Vorst, Marja M J; Knibbe, Catherijne A J; de Boer, Anthonius; Mantel-Teeuwisse, Aukje K

    2014-08-01

    A population-based cohort study was conducted in the Dutch PHARMO database to investigate prevalence and patterns of anti-infective medication use in children and adolescents with type 1 diabetes (T1D) before and after the onset of this disease. All patients <19 years with at least 2 insulin prescriptions (1999 to 2009) were identified (T1D cohort) and compared with an age- and sex-matched (ratio: 1 up to 4) diabetes-free reference group. The prevalence and average number of anti-infective use was studied from (up to) 8 years before until a maximum of 4 years after the onset of T1D. A total of 925 patients with T1D and 3,591 children and adolescents in the reference cohort (51% boys, mean age of 10.1 [standard deviation, 4.5] years) were included. The overall prevalence of anti-infective use (62.6 compared to 52.6%, P < 0.001) and average number of prescriptions (2.71 compared to 1.42 per child, P < 0.001) in the T1D cohort were significantly higher than those in the reference cohort after the onset of diabetes. This pattern was consistent across sex and age categories and already observed in the year before the onset of type 1 diabetes. Patients in the T1D cohort received more antibacterials (49.8 compared to 40%, P < 0.001), antimycotics (4.0 compared to 1.3%, P < 0.001), antivirals (2.5 compared to 0.4%, P < 0.001), and second-line antibiotics, such as aminoglycosides, quinolones, and third-generation cephalosporins and carbapenems. Our findings that elevated anti-infective use in the T1D cohort exists in the period before the onset of type 1 diabetes and the consumption of more second-line anti-infective compounds in this time period warrant further research.

  12. Modelling and comparison studies of packed screen regenerators for active magnetocaloric refrigeration

    DEFF Research Database (Denmark)

    Lei, Tian; Engelbrecht, Kurt; Nielsen, Kaspar Kirstein;

    2014-01-01

    In active magnetic regeneration (AMR) systems, not only the magnetocaloric properties of materials, but also the regenerator geometry plays an important role in the system performance. Packed sphere regenerators are often employed in existing prototypes, however, the characteristics such as relat......In active magnetic regeneration (AMR) systems, not only the magnetocaloric properties of materials, but also the regenerator geometry plays an important role in the system performance. Packed sphere regenerators are often employed in existing prototypes, however, the characteristics...... such as relatively large pressure drop and almost fixed porosity make loss reductions and further optimization challenging. This paper proposes and focuses on packed screen regenerators, which may exhibit lower pressure drop and equivalent heat transfer performance to packed sphere regenerators. A 1D AMR model...

  13. Screening of Taiwanese crude drugs for antibacterial activity against Streptococcus mutans.

    Science.gov (United States)

    Chen, C P; Lin, C C; Namba, T

    1989-12-01

    Preliminary antibacterial screening of local crude drugs was carried out using the cariogenic bacterium, Streptococcus mutans. Of 79 aqueous extracts tested, 6 crude drugs were shown to have significant antibacterial activity with minimal inhibitory concentration equal to or lower than 7.8 mg/ml (expressed in terms of dry starting material). Of these effective crude drugs, Morus australis, Ludwigia octovalvis and Thuja orientalis were very effective in inhibiting the growth of serotypes c and d of S. mutans (MIC less than or equal to 2.0-7.8 mg/ml). Elephantopus scaber, Artemisia vulgaris, Mosla chinensis and Orthosiphon aristatus also exhibited considerable antibacterial activity (MIC = 7.8-23.4 mg/ml) against both serotypes. In the presence of 5% sucrose, the antibacterial potency of the majority of the extracts did not change for type c, while the potency decreased about one-half for type d.

  14. Screening of Caesalpinia pulcherrima Linn Flowers for Analgesic and Anti-inflammatory Activities

    Directory of Open Access Journals (Sweden)

    S S Patel

    2010-09-01

    Full Text Available Summary: The flowers of Caesalpinia pulcherrima were extracted with methanol to determine their analgesic and anti-inflammatory activities. Intraperitoneal administration of methanolic extract (75, 150 and 225 mg/kg produced significant analgesic activity in acetic acid-induced writhing, tail immersion test and hot plate tests and anti-inflammatory effect against carrageenan-induced paw edema in experimental animals. Industrial relevance: The herbal medicines are getting more importance in the treatment of inflammation because of the side effect of the current therapy used to treat those inflammation using synthetic drugs. Herbal medicines have less side effects and less costly when compared to the synthetic drugs. The present study will help the industry to produce herbal drug with less side effect, less costly affordable and more effective in the treatment of pain and inflammation. Finally the phytochemical screening or elucidation of the bioactive compounds from the plant would be effective drug against pain and inflammation.

  15. Biological activity of Aronia melanocarpa antioxidants pre-screening in intervention study design

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    Konić-Ristić Aleksandra

    2013-01-01

    Full Text Available Beneficial effects of black chokeberry fruits and juices in health promotion and prevention of chronic diseases shown both in epidemiological and dietary intervention studies are often connected with their antioxidant activity. The aim of this study was to investigate the total phenolics and anthocyanins content, chemical antioxidant activity (DPPH-assay, antioxidant protection in erythrocytes and anti-platelet activity in vitro of three different chokeberry products: commercial and fresh pure chokeberry juice and crude lyophilized water-ethanol extract of chokeberry fruits, as a part of their pre-clinical evaluation. Obtained results indicated the differences in chemical composition and antioxidant activity of investigated products. Cellular effects, including both in vitro anti-platelet and antioxidant effects, were not directly correlated with the chemical antioxidant activity and results obtained in vitro for anti-platelet effects just partially consistent with the results obtained in vivo, in a pilot intervention trial. In conclusion, chemical analyses and in vitro experiments on foods and their bioactives are a valuable pre-screening tool for the evaluation of their biological activity. However, extrapolation of the obtained results to the in vivo settings is often limited and influenced by the bioavailability and metabolism of native dietary compounds or interactions with different molecules within the human body. [Projekat Ministarstva nauke Republike Srbije, br. III41030

  16. Quantitative high-throughput screening identifies 8-hydroxyquinolines as cell-active histone demethylase inhibitors.

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    Oliver N F King

    Full Text Available BACKGROUND: Small molecule modulators of epigenetic processes are currently sought as basic probes for biochemical mechanisms, and as starting points for development of therapeutic agents. N(ε-Methylation of lysine residues on histone tails is one of a number of post-translational modifications that together enable transcriptional regulation. Histone lysine demethylases antagonize the action of histone methyltransferases in a site- and methylation state-specific manner. N(ε-Methyllysine demethylases that use 2-oxoglutarate as co-factor are associated with diverse human diseases, including cancer, inflammation and X-linked mental retardation; they are proposed as targets for the therapeutic modulation of transcription. There are few reports on the identification of templates that are amenable to development as potent inhibitors in vivo and large diverse collections have yet to be exploited for the discovery of demethylase inhibitors. PRINCIPAL FINDINGS: High-throughput screening of a ∼236,000-member collection of diverse molecules arrayed as dilution series was used to identify inhibitors of the JMJD2 (KDM4 family of 2-oxoglutarate-dependent histone demethylases. Initial screening hits were prioritized by a combination of cheminformatics, counterscreening using a coupled assay enzyme, and orthogonal confirmatory detection of inhibition by mass spectrometric assays. Follow-up studies were carried out on one of the series identified, 8-hydroxyquinolines, which were shown by crystallographic analyses to inhibit by binding to the active site Fe(II and to modulate demethylation at the H3K9 locus in a cell-based assay. CONCLUSIONS: These studies demonstrate that diverse compound screening can yield novel inhibitors of 2OG dependent histone demethylases and provide starting points for the development of potent and selective agents to interrogate epigenetic regulation.

  17. In vivo screening of essential oils of Skimmia laureola leaves for antinociceptive and antipyretic activity

    Institute of Scientific and Technical Information of China (English)

    Naveed Muhammad; Barkatullah; Muhammad Ibrar; Haroon Khan; Muhammad Saeed; Amir Zada Khan; Waqar Ahmad Kaleem

    2013-01-01

    Objective:To study the screening of essential oils of Skimmia laureola leaves (SLO) for acute toxicity, antinociceptive, antipyretic and anticonvulsant activities in various animal models. Methods: SLO were extracted using modified Clevenger type apparatus. Acute toxicity test was used in mice to observe its safety level. Antinociceptive activity of SLO was evaluated in acetic acid induced writhing and hot plate tests. Yeast induced hyperthermic mice and pentylenetetrazole induced convulsive mice were used for the assessment of its antipyretic and anticonvulsant profile respectively. Results: Substantial safety was observed for SLO in acute toxicity test. SLO showed a high significant activity in acetic acid induced writhing test in a dose dependent manner with maximum pain attenuation of 68.48%at 200 mg/kg i.p. However, it did not produce any relief in thermal induced pain at test doses. When challenged against pyrexia evoked by yeast, SLO manifested marked amelioration in hyperthermic mice, dose dependently. Maximum anti-hyperthermic activity (75%) was observed at 200 mg/kg i.p. after 4 h of drug administration. Nevertheless, SLO had no effect on seizures control and mortality caused by pentylenetetrazole. Conclusions:In vivo studies of SLO showed prominent antinociceptive and antipyretic activities with ample safety profile and thus provided pharmacological base for the traditional uses of the plant in various painful conditions and pyrexia. Additional detail studies are required to ascertain its clinical application.

  18. Screening of vasorelaxant activity of some medicinal plants used in Oriental medicines.

    Science.gov (United States)

    Yin, Ming Hao; Kang, Dae Gill; Choi, Deok Ho; Kwon, Tae Oh; Lee, Ho Sub

    2005-05-13

    Hexane, ethylacetate (EtOAC), and n-butanol (n-BuOH) extracts of medicinal plants traditionally used in the East Asia, such as China, Korea, and Japan were screened for their vasorelaxant activity using isolated rat aorta. Among the 60 solvent-extracts from 20 medicinal plants, hexane and n-BuOH extracts of Diospyros kaki and Polygonum aviculare, hexane, EtOAC, and n-BuOH extracts of Magnolia liliflora, n-BuOH extract of Sorbus commixta, and EtOAC and n-BuOH extracts of Selaginella tamariscina were found to exhibit distinctive vasorelaxant activity. The activity disappeared by removal of functional endothelium or pre-treatment of the aortic tissues with N(G)-nitro-L-arginine methyl ester (L-NAME), which is an inhibitor of nitric oxide synthase. These findings suggest that the medicinal plants relax vascular smooth muscle via endothelium-dependent nitric oxide. These results will be useful to further analyze those medicinal plants that contain the vasorelaxant activity in order to identify the active principles.

  19. SCREENING OF ANTIMICROBIAL ACTIVITY AND GENES CODING POLYKETIDE SYNTHETASE AND NONRIBOSOMAL PEPTIDE SYNTHETASE OF ACTINOMYCETE ISOLATES

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    Silvia Kovácsová

    2013-12-01

    Full Text Available The aim of this study was to observe antimicrobial activity using agar plate diffusion method and screening genes coding polyketide synthetase (PKS-I and nonribosomal peptide synthetase (NRPS from actinomycetes. A total of 105 actinomycete strains were isolated from arable soil. Antimicrobial activity was demonstrated at 54 strains against at least 1 of total 12 indicator organisms. Antifungal properties were recorded more often than antibacterial properties. The presence of PKS-I and NRPS genes were founded at 61 of total 105 strains. The number of strains with mentioned biosynthetic enzyme gene fragments matching the anticipated length were 19 (18% and 50 (47% respectively. Overall, five actinomycete strains carried all the biosynthetical genes, yet no antimicrobial activity was found against any of tested pathogens. On the other hand, twenty-one strains showed antimicrobial activity even though we were not able to amplify any of the PKS or NRPS genes from them. Combination of the two methods showed broad-spectrum antimicrobial activity of actinomycetes isolated from arable soil, which indicate that actinomycetes are valuable reservoirs of novel bioactive compounds.

  20. Colorimetry and SERS dual-mode detection of telomerase activity: combining rapid screening with high sensitivity

    Science.gov (United States)

    Zong, Shenfei; Wang, Zhuyuan; Chen, Hui; Hu, Guohua; Liu, Min; Chen, Peng; Cui, Yiping

    2014-01-01

    As an important biomarker and therapeutic target, telomerase has attracted considerable attention concerning its detection and monitoring. Here, we present a colorimetry and surface enhanced Raman scattering (SERS) dual-mode telomerase activity detection method, which has several distinctive advantages. First, colorimetric functionality allows rapid preliminary discrimination of telomerase activity by the naked eye. Second, the employment of SERS technique results in greatly improved detection sensitivity. Third, the combination of colorimetry and SERS into one detection system can ensure highly efficacious and sensitive screening of numerous samples. Besides, the avoidance of polymerase chain reaction (PCR) procedures further guarantees fine reliability and simplicity. Generally, the presented method is realized by an ``elongate and capture'' procedure. To be specific, gold nanoparticles modified with Raman molecules and telomeric repeat complementary oligonucleotide are employed as the colorimetric-SERS bifunctional reporting nanotag, while magnetic nanoparticles functionalized with telomerase substrate oligonucleotide are used as the capturing substrate. Telomerase can synthesize and elongate telomeric repeats onto the capturing substrate. The elongated telomeric repeats subsequently facilitate capturing of the reporting nanotag via hybridization between telomeric repeat and its complementary strand. The captured nanotags can cause a significant difference in the color and SERS intensity of the magnetically separated sediments. Thus both the color and SERS can be used as indicators of the telomerase activity. With fast screening ability and outstanding sensitivity, we anticipate that this method would greatly promote practical application of telomerase-based early-stage cancer diagnosis.As an important biomarker and therapeutic target, telomerase has attracted considerable attention concerning its detection and monitoring. Here, we present a colorimetry and

  1. Parenting style, the home environment, and screen time of 5-year-old children; the 'be active, eat right' study.

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    Lydian Veldhuis

    Full Text Available INTRODUCTION: The global increase in childhood overweight and obesity has been ascribed partly to increases in children's screen time. Parents have a large influence on their children's screen time. Studies investigating parenting and early childhood screen time are limited. In this study, we investigated associations of parenting style and the social and physical home environment on watching TV and using computers or game consoles among 5-year-old children. METHODS: This study uses baseline data concerning 5-year-old children (n = 3067 collected for the 'Be active, eat right' study. RESULTS: Children of parents with a higher score on the parenting style dimension involvement, were more likely to spend >30 min/day on computers or game consoles. Overall, families with an authoritative or authoritarian parenting style had lower percentages of children's screen time compared to families with an indulgent or neglectful style, but no significant difference in OR was found. In families with rules about screen time, children were less likely to watch TV>2 hrs/day and more likely to spend >30 min/day on computers or game consoles. The number of TVs and computers or game consoles in the household was positively associated with screen time, and children with a TV or computer or game console in their bedroom were more likely to watch TV>2 hrs/day or spend >30 min/day on computers or game consoles. CONCLUSION: The magnitude of the association between parenting style and screen time of 5-year-olds was found to be relatively modest. The associations found between the social and physical environment and children's screen time are independent of parenting style. Interventions to reduce children's screen time might be most effective when they support parents specifically with introducing family rules related to screen time and prevent the presence of a TV or computer or game console in the child's room.

  2. Virtual Screening Analysis and In-vitro Xanthine Oxidase Inhibitory Activity of Some Commercially Available Flavonoids.

    Science.gov (United States)

    Umamaheswari, Muthuswamy; Madeswaran, Arumugam; Asokkumar, Kuppusamy

    2013-01-01

    Allopurinol, the xanthine oxidase inhibitor, is the only drug available for the treatment of gout. We examined the xanthine oxidase inhibitory activity of some commercially available flavonoids such asepigallocatechin, acacatechin, myricetin, naringenin, daidzein and glycitein by virtual screening and in-vitro studies. The interacting residues within the complex model and their contact types were identified. The virtual screening analysis were carried out using AutoDock 4.2 and in-vitro xanthine oxidase inhibitory activity was carried out using xanthine as the substrate. In addition, enzyme kinetics was performed using LineweaverBurkplot analysis. Allopurinol, a known xanthine oxidase inhibitor was used as the standard. The docking energy ofglycitein was found to be -8.49 kcal/mol which was less than that of the standard (-4.47 kcal/ mol). All the selected flavonoids were found to exhibit lower binding energy (-8.08 to -6.03 kcal/ mol) than allopurinol. The docking results confirm that flavonoids showed greater inhibition of xanthine oxidase due to their active binding sites and lesser binding energies compared to allopurinol. This may be attributed to the presence of benzopyran ring in the flavonoids. In the xanthine oxidase assay, IC50 value of glycitein was found to be 12±0.86 μg/mL, whereas that of allopurinol was 24±0.28 μg/mL. All the remaining compounds exhibited IC50 values ranging between 22±0.64 to 62±1.18 μg/mL. In the enzyme kinetic studies, flavonoids showed competitive type of enzyme inhibition. It can be concluded that flavonoids could be a promising remedy for the treatment of gout and related inflammatory disorders. Further in-vivo studies are required to develop potential compounds with lesser side effects. PMID:24250638

  3. Community-based screening for pre-hypertension among military active duty personnel

    Institute of Scientific and Technical Information of China (English)

    Moataz M. Abdel-Fattah; Fayssal M. Farahat; Abdul-Salam A. Al-Shehri

    2009-01-01

    Objective: The purpose of this study to determine the prevalence of both pre-hypertension and hypertension and risk factors associated with newly diagnosed Saudi military active duty service personnel. Methods: Community-based screening of 1283 Saudi military active duty service personnel was conducted during the period September - December 2007 at six randomly selected out of a total of 15 military units of Taif region, Western of Saudi Arabia. Screening tools included self-administrated questionnaire, general physical examination, anthropometric measurements and assessment of blood pressure. Results: All par-ticipants were Saudi males. Their age ranged from 19-56 years old with mean ± SD of 37.2 ± 7.02. By applying the Joint Na-tional Committee on prevention, detection, evaluation, and treatment of high hypertension (JNC-7) criteria, 214 ( 17.3 % ) were considered pre-hypertensive. Multivariate logistic regression analysis showed that obesity as measured by body mass index ( OR = 2.71 CI: 1.39-5.28 ), positive family history ( OR = 1.46 CI: 1.03-2.06 ), ever smoking ( OR = 1.45 CI: 1.05-2.02), and in-creased waist circumference ( OR = 1.04 CI:1. 02-1.06) were the significant predictors of workplace newly diagnosed hyperten-sion among military active duty personnel. Conclusion: Pre-hypertension is a common hidden problem and it predicts the devel-opment of frank hypertension. Findings of the current study support the recommendation of lifestyle modification for pre-hyperten-sion patients. However, further prospective studied are required to determine the role of pharmacotherapy in pre-hypertension.

  4. Active renin mass concentration to determine aldosterone-to-renin ratio in screening for primary aldosteronism

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    Corbin F

    2011-07-01

    Full Text Available François Corbin1, Pierre Douville2, Marcel Lebel3 1Division of Biochemistry, l'Université de Sherbrooke, Sherbrooke, Quebec, Canada; 2Division of Biochemistry; 3Division of Nephrology, L'Hôtel-Dieu de Québec Hospital and l'Université Laval, Quebec, CanadaBackground: Active renin mass concentration (ARC is independent of the endogenous level of angiotensinogen, and less variable and more reproducible than plasma renin activity. Reference values for the aldosterone-to-renin ratio (ARR using ARC are still undefined. The objective of the present study was to determine the threshold of ARR using ARC measurement to screen for primary aldosteronism.Methods: A total of 211 subjects were included in the study, comprising 78 healthy normotensive controls, 95 patients with essential hypertension, and 38 patients with confirmed primary aldosteronism (20 with surgery-confirmed aldosterone-producing adenoma and 18 with idiopathic adrenal hyperplasia. Blood samples were drawn from ambulatory patients and volunteers in the mid-morning without specific dietary restriction for measuring plasma aldosterone concentration, ARC, and serum potassium.Results: Most normotensive controls and essential hypertension patients had ARR results below 100 pmol/ng, a value which corresponded to 3.3 times the median of these two groups.Conclusion: Patients with ARR values above this level should be considered for further investigation (confirmatory tests or for repeat testing should ARR values be borderline. This study indicates that ARC can be used reliably in determining ARR for primary aldosteronism screening.Keywords: primary aldosteronism, active renin mass concentration, aldosterone-to-renin ratio

  5. Screening of medicinal plants for induction of somatic segregation activity in Aspergillus nidulans.

    Science.gov (United States)

    Ramos Ruiz, A; De la Torre, R A; Alonso, N; Villaescusa, A; Betancourt, J; Vizoso, A

    1996-07-01

    Knowledge about mutagenic properties of plants commonly used in traditional medicine is limited. A screening for genotoxic activity was carried out in aqueous or alcoholic extracts prepared from 13 medicinal plants widely used as folk medicine in Cuba: Lepidium virginicum L. (Brassicaceae): Plantago major L. and Plantago lanceolata L. (Plantaginaceae); Ortosiphon aristatus Blume, Mentha x piperita L., Melissa officinalis L. and Plectranthus amboinicus (Lour.) Spreng. (Lamiaceae); Cymbopogon citratus (DC.) Stapf (Poaceae); Passiflora incarnata L. (Passifloraceae); Zingiber officinale Roscoe (Zingiberaceae); Piper auritum HBK. (Piperaceae); Schinus terebinthifolius Raddi (Anacardeaceae) and Momordica charantia L. (Cucurbitaceae). A plate incorporation assay with Aspergillus nidulans was employed, allowing detection of somatic segregation as a result of mitotic crossing-over, chromosome malsegregation or clastogenic effects. Aspergillus nidulans D-30, a well-marked strain carrying four recessive mutations for conidial color in heterozygosity, which permitted the direct visual detection of segregants, was used throughout this study. As a result, only in the aqueous extract of one of the plants screened (Momordica charantia) a statistical significant increase in the frequency of segregant sectors per colony was observed, and consequently, a genotoxic effect is postulated.

  6. Screening of Lignocellulose-Degrading Superior Mushroom Strains and Determination of Their CMCase and Laccase Activity

    Directory of Open Access Journals (Sweden)

    Li Fen

    2014-01-01

    Full Text Available In order to screen lignocellulose-degrading superior mushroom strains ten strains of mushrooms (Lentinus edodes939, Pholiota nameko, Lentinus edodes868, Coprinus comatus, Macrolepiota procera, Auricularia auricula, Hericium erinaceus, Grifola frondosa, Pleurotus nebrodensis, and Shiraia bambusicola were inoculated onto carboxymethylcellulose agar-Congo red plates to evaluate their ability to produce carbomethyl cellulase (CMCase. The results showed that the ratio of transparent circle to mycelium circle of Hericium erinaceus was 8.16 (P<0.01 higher than other strains. The filter paper culture screening test showed that Hericium erinaceus and Macrolepiota procera grew well and showed extreme decomposition of the filter paper. When cultivated in guaiacol culture medium to detect their abilities to secrete laccase, Hericium erinaceus showed the highest ability with the largest reddish brown circles of 4.330 cm. CMCase activity determination indicated that Coprinus comatus and Hericium erinaceus had the ability to produce CMCase with 33.92 U/L on the 9th day and 22.58 U/L on the 10th day, respectively, while Coprinus comatus and Pleurotus nebrodensis had the ability to produce laccase with 496.67 U/L and 489.17 U/L on the 16th day and 18th day. Based on the results, Coprinus comatus might be the most promising lignocellulose-degrading strain to produce both CMCase and laccase at high levels.

  7. [Cardiovascular screening for recreational, leisure, vigorous and competitive sport activities over 35 years].

    Science.gov (United States)

    Leischik, R; Littwitz, H; Dworrak, B; Spelsberg, N; Seyfarth, M; Tiroch, K

    2014-10-01

    Particularly among over 30 years old ambitious hobby- and competitive athletes arrhythmias and even sudden cardiac deaths occur again and again. The spectacular sudden deaths during marathon, football and, just recently, in the trend discipline triathlon seem to support that view. Reports about the "athlete`s heart" and complications in the elderly causes uncertainty among athletes, fitness fans and sports physicians. The question arises, how to avoid complications caused by ambitious sporting activity in the elderly and how to screen hobby- and ambitious athletes between the age of 35 and 75 years. For athletes > 35 years old besides medical history and physical examination basic examinations including resting ECG, echocardiography and exercise ECG/stress echocardiography are mandatory. Further examinations, if clinically necessary, should be spiroergometry, Holter ECG or magnetic resonance tomography and Carotis-Duplex or Cardio-CT for the purpose of arteriosclerosis screening. In suspicious inflammation a further extended laboratory testing may become necessary (incl. viral/bacterial antibodies) or even a multidisciplinary approach (immunological, neurological, dental or orthodontic examination).

  8. Screening of medicinal plants for induction of somatic segregation activity in Aspergillus nidulans.

    Science.gov (United States)

    Ramos Ruiz, A; De la Torre, R A; Alonso, N; Villaescusa, A; Betancourt, J; Vizoso, A

    1996-07-01

    Knowledge about mutagenic properties of plants commonly used in traditional medicine is limited. A screening for genotoxic activity was carried out in aqueous or alcoholic extracts prepared from 13 medicinal plants widely used as folk medicine in Cuba: Lepidium virginicum L. (Brassicaceae): Plantago major L. and Plantago lanceolata L. (Plantaginaceae); Ortosiphon aristatus Blume, Mentha x piperita L., Melissa officinalis L. and Plectranthus amboinicus (Lour.) Spreng. (Lamiaceae); Cymbopogon citratus (DC.) Stapf (Poaceae); Passiflora incarnata L. (Passifloraceae); Zingiber officinale Roscoe (Zingiberaceae); Piper auritum HBK. (Piperaceae); Schinus terebinthifolius Raddi (Anacardeaceae) and Momordica charantia L. (Cucurbitaceae). A plate incorporation assay with Aspergillus nidulans was employed, allowing detection of somatic segregation as a result of mitotic crossing-over, chromosome malsegregation or clastogenic effects. Aspergillus nidulans D-30, a well-marked strain carrying four recessive mutations for conidial color in heterozygosity, which permitted the direct visual detection of segregants, was used throughout this study. As a result, only in the aqueous extract of one of the plants screened (Momordica charantia) a statistical significant increase in the frequency of segregant sectors per colony was observed, and consequently, a genotoxic effect is postulated. PMID:8771452

  9. Plasma nitriding monitoring reactor: A model reactor for studying plasma nitriding processes using an active screen

    Science.gov (United States)

    Hamann, S.; Börner, K.; Burlacov, I.; Spies, H.-J.; Strämke, M.; Strämke, S.; Röpcke, J.

    2015-12-01

    A laboratory scale plasma nitriding monitoring reactor (PLANIMOR) has been designed to study the basics of active screen plasma nitriding (ASPN) processes. PLANIMOR consists of a tube reactor vessel, made of borosilicate glass, enabling optical emission spectroscopy (OES) and infrared absorption spectroscopy. The linear setup of the electrode system of the reactor has the advantages to apply the diagnostic approaches on each part of the plasma process, separately. Furthermore, possible changes of the electrical field and of the heat generation, as they could appear in down-scaled cylindrical ASPN reactors, are avoided. PLANIMOR has been used for the nitriding of steel samples, achieving similar results as in an industrial scale ASPN reactor. A compact spectrometer using an external cavity quantum cascade laser combined with an optical multi-pass cell has been applied for the detection of molecular reaction products. This allowed the determination of the concentrations of four stable molecular species (CH4, C2H2, HCN, and NH3). With the help of OES, the rotational temperature of the screen plasma could be determined.

  10. Plasma nitriding monitoring reactor: A model reactor for studying plasma nitriding processes using an active screen

    Energy Technology Data Exchange (ETDEWEB)

    Hamann, S., E-mail: hamann@inp-greifswald.de; Röpcke, J. [INP-Greifswald, Felix-Hausdorff-Str. 2, 17489 Greifswald (Germany); Börner, K.; Burlacov, I.; Spies, H.-J. [TU Bergakademie Freiberg, Institute of Materials Engineering, Gustav-Zeuner-Str. 5, 09599 Freiberg (Germany); Strämke, M.; Strämke, S. [ELTRO GmbH, Arnold-Sommerfeld-Ring 3, 52499 Baesweiler (Germany)

    2015-12-15

    A laboratory scale plasma nitriding monitoring reactor (PLANIMOR) has been designed to study the basics of active screen plasma nitriding (ASPN) processes. PLANIMOR consists of a tube reactor vessel, made of borosilicate glass, enabling optical emission spectroscopy (OES) and infrared absorption spectroscopy. The linear setup of the electrode system of the reactor has the advantages to apply the diagnostic approaches on each part of the plasma process, separately. Furthermore, possible changes of the electrical field and of the heat generation, as they could appear in down-scaled cylindrical ASPN reactors, are avoided. PLANIMOR has been used for the nitriding of steel samples, achieving similar results as in an industrial scale ASPN reactor. A compact spectrometer using an external cavity quantum cascade laser combined with an optical multi-pass cell has been applied for the detection of molecular reaction products. This allowed the determination of the concentrations of four stable molecular species (CH{sub 4}, C{sub 2}H{sub 2}, HCN, and NH{sub 3}). With the help of OES, the rotational temperature of the screen plasma could be determined.

  11. Yeast-Based High-Throughput Screens to Identify Novel Compounds Active against Brugia malayi.

    Directory of Open Access Journals (Sweden)

    Elizabeth Bilsland

    2016-01-01

    Full Text Available Lymphatic filariasis is caused by the parasitic worms Wuchereria bancrofti, Brugia malayi or B. timori, which are transmitted via the bites from infected mosquitoes. Once in the human body, the parasites develop into adult worms in the lymphatic vessels, causing severe damage and swelling of the affected tissues. According to the World Health Organization, over 1.2 billion people in 58 countries are at risk of contracting lymphatic filariasis. Very few drugs are available to treat patients infected with these parasites, and these have low efficacy against the adult stages of the worms, which can live for 7-15 years in the human body. The requirement for annual treatment increases the risk of drug-resistant worms emerging, making it imperative to develop new drugs against these devastating diseases.We have developed a yeast-based, high-throughput screening system whereby essential yeast genes are replaced with their filarial or human counterparts. These strains are labeled with different fluorescent proteins to allow the simultaneous monitoring of strains with parasite or human genes in competition, and hence the identification of compounds that inhibit the parasite target without affecting its human ortholog. We constructed yeast strains expressing eight different Brugia malayi drug targets (as well as seven of their human counterparts, and performed medium-throughput drug screens for compounds that specifically inhibit the parasite enzymes. Using the Malaria Box collection (400 compounds, we identified nine filarial specific inhibitors and confirmed the antifilarial activity of five of these using in vitro assays against Brugia pahangi.We were able to functionally complement yeast deletions with eight different Brugia malayi enzymes that represent potential drug targets. We demonstrated that our yeast-based screening platform is efficient in identifying compounds that can discriminate between human and filarial enzymes. Hence, we are confident

  12. Is spending time in screen-based sedentary behaviors associated with less physical activity: a cross national investigation

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    Iannotti Ronald J

    2010-05-01

    Full Text Available Abstract Background In Australia and the USA, national guidelines exist for limiting children's screen-exposure to two hours per day. This study aims to determine whether exceeding the suggested guidelines for screen-based sedentary behavior is associated with reduced levels of physical activity across different geographical regions. Methods Data material were taken from the 2005/2006 survey of "Health Behaviour in School-aged Children (HBSC study; A WHO cross-National Survey". Data were collected through questionnaires from 11-,13- and,15- year olds. The final sample included 200,615 adolescents from 39 different countries in Europe and North America. Gender and country stratified analyses regressed time spent in leisure-time vigorous physical activity (VPA and days of 60 minutes moderate to vigorous physical activity (MVPA on time spent in screen-based sedentary behaviors. To simplify interpretation, the estimates from each country were pooled using a meta-analytic procedure. Results Exceeding 2 hrs of daily total screen-time was negatively associated with MVPA for both boys and girls, and with VPA for girls. When investigating the different types of screen-based behaviors separately, exceeding 2 hrs daily of TV viewing was associated with less MVPA for both boys and girls and less VPA for girls. Gaming was associated with less MVPA and VPA for boys, and non-gaming computer use was associated with higher levels of VPA for both genders. Stronger negative associations between physical activity and screen-based sedentary behaviors were found in countries where mean levels of physical activity were relatively high. The association between physical activity and sedentary behavior was not significantly associated with national levels of screen-based sedentary behaviors. Conclusions The displacement mechanism does not appear to be universal across countries. On a national level, negative associations between physical activity and screen

  13. SCREENING FOR ANTIMICROBIAL ACTIVITY AND PHYTOCHEMICAL ANALYSIS OF VARIOUS LEAF EXTRACT OF MURRAYA KOENIGII

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    C. Baskaran

    2011-06-01

    Full Text Available To investigate the antimicrobial activity and phytochemical screening Ethanol, methanol, Ethyl acetate, aceton,chloroform, Petroleum ether, hexane, hot water, and extracts of Murraya koenigii. The aim of the present study was to evaluate the qualitative analysis of phytochemicals and antimicrobial activity of various solvent extracts of Murraya koenigii. The antimicrobial activity of different solvent extracts of Murraya koenigii were tested against the Gram-positive and Gram-negative bacterial strains and fungus by observing the zone of inhibition. The Gram-positive bacteria used in the test were Staphylococcus aureus, Bacillus cereus and Micrococcus luteus, and the Gram-negative bacteria were Escherichia coli, Pseudomonas aeruginosa and Klebsiella pneumoniae, fungus like Aspergillus niger, Candida albicans, Candida tropicalis, Cryptococcus neoformans and Candida kefyr. It was observed that ethanol, methanol, ethyl acetate, aceton, chloroform, petroleum ether, hexane and aquas extracts showed activity against bacteria and fungus. The Hot water extract of Murraya koenigii showed more activity against Staphylococcus aureus, zone of diameter 28.17±0.29mm and Ethanol extract of Murraya koenigii showed more activity against Aspergillus niger and Candida tropicalis, zone of diameter 12.17±0.15mm compared to other solvent extracts. In this study Hot water Extract in bacteria and Ethanol Extract in fungus showed a varying degree of inhibition to the growth of tested organism, than methanol, Ethyl acetate, aceton, chloroform, Petroleum ether, hexane, and acetone extracts, The results confirmed the presence of antibacterial activity of Murraya koenigii extract against various human pathogenic bacteria. Presences of phytochemical and antimicrobial activity are confirmed.

  14. Combined Rational Design and a High Throughput Screening Platform for Identifying Chemical Inhibitors of a Ras-activating Enzyme*

    Science.gov (United States)

    Evelyn, Chris R.; Biesiada, Jacek; Duan, Xin; Tang, Hong; Shang, Xun; Papoian, Ruben; Seibel, William L.; Nelson, Sandra; Meller, Jaroslaw; Zheng, Yi

    2015-01-01

    The Ras family small GTPases regulate multiple cellular processes, including cell growth, survival, movement, and gene expression, and are intimately involved in cancer pathogenesis. Activation of these small GTPases is catalyzed by a special class of enzymes, termed guanine nucleotide exchange factors (GEFs). Herein, we developed a small molecule screening platform for identifying lead hits targeting a Ras GEF enzyme, SOS1. We employed an ensemble structure-based virtual screening approach in combination with a multiple tier high throughput experimental screen utilizing two complementary fluorescent guanine nucleotide exchange assays to identify small molecule inhibitors of GEF catalytic activity toward Ras. From a library of 350,000 compounds, we selected a set of 418 candidate compounds predicted to disrupt the GEF-Ras interaction, of which dual wavelength GDP dissociation and GTP-loading experimental screening identified two chemically distinct small molecule inhibitors. Subsequent biochemical validations indicate that they are capable of dose-dependently inhibiting GEF catalytic activity, binding to SOS1 with micromolar affinity, and disrupting GEF-Ras interaction. Mutagenesis studies in conjunction with structure-activity relationship studies mapped both compounds to different sites in the catalytic pocket, and both inhibited Ras signaling in cells. The unique screening platform established here for targeting Ras GEF enzymes could be broadly useful for identifying lead inhibitors for a variety of small GTPase-activating GEF reactions. PMID:25825487

  15. Screening for estrogenic and antiestrogenic activities of plants growing in Egypt and Thailand

    Directory of Open Access Journals (Sweden)

    Ali M El-Halawany

    2011-01-01

    Full Text Available Background: There is a growing demand for the discovery of new phytoestrogens to be used as a safe and effective hormonal replacement therapy. Materials and Methods: The methanol extracts of 40 plants from the Egyptian and Thailand folk medicines were screened for their estrogen agonist and antagonist activities. The estrogenic and antiestrogenic effects of the tested extracts were carried out using the yeast two-hybrid assay system expressing ERα and ERβ. In addition, all the extracts were subjected to a naringinase treatment and retested for their estrogenic activity. Results: The methanol extracts of Derris reticulata and Dracaena lourieri showed the most potent estrogenic activity on both estrogen-receptor subtypes, while, the methanol extracts of Butea monosperma, Erythrina fusca, and Dalbergia candenatensis revealed significant estrogenic activity on ERβ only. Nigella sativa, Sophora japonica, Artabotrys harmandii, and Clitorea hanceana showed estrogenic effect only after naringinase treatment. The most potent antiestrogenic effect was revealed by Aframomum melegueta, Dalbergia candenatensis, Dracena loureiri, and Mansonia gagei.

  16. Phytochemical screening, cytotoxicity and antibacterial activities of two Bangladeshi medicinal plants.

    Science.gov (United States)

    Roy, Ajoy; Biswas, Subrata Kumar; Chowdhury, Anusua; Shill, Manik Chandra; Raihan, Sheikh Zahir; Muhit, Md Abdul

    2011-10-01

    The objectives of the present study were to investigate phytochemical screening and to assay cytotoxicity and antibacterial activities of ethanolic extracts of leaves of two medicinal plants, Aglaonema hookerianum Schott (Family: Araceae) and Lannea grandis Engl. (Family: Anacardiaceae) available in Bangladesh. The brine shrimp lethality bioassay showed that the ethanolic extracts of Aglaonema hookerianum and Lannea grandis possessed cytotoxic activities with LC50 5.25 (microg mL(-1)) and 5.75 (microg mL(-1)) and LC90 10.47 (microg mL(-1)) and 9.55 (microg mL(-1)), respectively. Two extracts obtained from leaves were examined for their antibacterial activities against some gram positive bacteria such as Bacillus subtilis, Bacillus megaterium and Staphylococcus aureus, also gram negative strains of Pseudomonas aeruginosa, Escherichia coli, Shigella dysenteriae, Salmonella typhi, Salmonella paratyphi and Vibrio cholerae. Agar disc diffusion method was applied to observe the antibacterial efficacy of the extracts. Results indicated that both plant extracts (500 microg disc(-1)) displayed antibacterial activity against all of the tested microorganisms. These results were also compared with the zones of inhibition produced by commercially available standard antibiotic, Amoxicillin at concentration of 10 microg disc(-1). Observed antibacterial properties of the ethanolic extract of Aglaonema hookerianum Schott and Lannea grandis Engl. showed that both plants might be useful sources for the development of new potent antibacterial agents.

  17. Screening of some Tanzanian medicinal plants for their trypanocidal and cytotoxic activities.

    Science.gov (United States)

    Nibret, Endalkachew; Ashour, Mohamed L; Rubanza, Chrispinus D; Wink, Michael

    2010-06-01

    The objective of the present study was to evaluate in vitro antitrypanosomal and cytotoxic activities of crude extracts of 20 traditionally used medicinal plants of Tanzania. A total of 40 extracts (dichloromethane and methanol) were screened for antiproliferative activity of bloodstream form of T. b. brucei and human leukaemia HL-60 cell. Inhibition of cell proliferation was assessed using resazurin as vital stain. Of the 40 extracts tested, the dichloromethane extract from bark of Warburgia salutaris (Canellaceae) exhibited the most potent antitrypanosomal activity with an IC(50) value of 10.68 microg/ml. A dichloromethane extract from Lannea stuhlmannii (Anacardiaceae) was found to be the most cytotoxic extract against HL-60 (IC(50) = 27.15 microg/ml). Out of the 20 plants tested, 5 plants exhibited trypanocidal activity with IC(50) values below 20 microg/ml. These 5 plants: Entandrophragma bussei (Meliaceae), Securidaca longepedunculata (Polygalaceae), Warburgia salutaris (Canellaceae), Zanha africana (Sapindaceae) and Zanthoxylum chalybeum (Rutaceae) could therefore serve as sources of lead compounds for treatment of trypanosomiasis. PMID:19957246

  18. Screening of Bothrops snake venoms for L-amino acid oxidase activity

    Energy Technology Data Exchange (ETDEWEB)

    Pessati, M.L.; Fontana, J.D.; Guimaraes, M.F. [Federal Univ. of Parana, Curitiba (Brazil)

    1995-12-31

    Toxins, enzymes, and biologically active peptides are the main components of snake venoms from the genus Bothrops. Following the venom inoculation, the local effects are hemorrhage, edema, and myonecrosis. Nineteen different species of Brazilian Bothrops were screened for protein content and L-amino acid oxidase activity. B. cotiara, formerly found in the South of Brazil, is now threatened with extinction. Its venom contains a highly hemorrhagic fraction and, as expected from the deep yellow color of the corresponding lyophilized powder, a high L-amino acid oxidase (LAO) activity was also characterized. Flavin adenine dinucleotide (FAD) is its associate coenzyme. B. cotiara venom LAO catalyzed the oxidative deamination of several L-amino acids, and the best substrates were methionine, leucine, tryptophan, and phenylalanine, hence, its potential application for the use in biosensors for aspartame determination and for the removal of amino acids from plasma. High levels for LAO were also found in other species than B. cotiara. In addition, the technique of isoelectric focusing (IEF) was employed as a powerful tool to study the iso- or multi-enzyme distribution for LAO activity in the B. cotiara snake venom.

  19. Screening and characterization of molecules that modulate the biological activity of IFNs-I.

    Science.gov (United States)

    Bürgi, Milagros; Zapol'skii, Viktor A; Hinkelmann, Bettina; Köster, Mario; Kaufmann, Dieter E; Sasse, Florenz; Hauser, Hansjörg; Etcheverrigaray, Marina; Kratje, Ricardo; Bollati-Fogolín, Mariela; Oggero, Marcos

    2016-09-10

    Type I Interferons (IFNs-I) are species-specific glycoproteins which play an important role as primary defence against viral infections and that can also modulate the adaptive immune system. In some autoimmune diseases, interferons (IFNs) are over-produced. IFNs are widely used as biopharmaceuticals for a variety of cancer indications, chronic viral diseases, and for their immuno-modulatory action in patients with multiple sclerosis; therefore, increasing their therapeutic efficiency and decreasing their side effects is of high clinical value. In this sense, it is interesting to find molecules that can modulate the activity of IFNs. In order to achieve that, it was necessary to establish a simple, fast and robust assay to analyze numerous compounds simultaneously. We developed four reporter gene assays (RGAs) to identify IFN activity modulator compounds by using WISH-Mx2/EGFP, HeLa-Mx2/EGFP, A549-Mx2/EGFP, and HEp2-Mx2/EGFP reporter cell lines (RCLs). All of them present a Z' factor higher than 0.7. By using these RGAs, natural and synthetic compounds were analyzed simultaneously. A total of 442 compounds were studied by the Low Throughput Screening (LTS) assay using the four RCLs to discriminate between their inhibitory or enhancing effects on IFN activity. Some of them were characterized and 15 leads were identified. Finally, one promising candidate with enhancing effect on IFN-α/-β activity and five compounds with inhibitory effect were described. PMID:27346232

  20. Screening of selected pesticides for inhibition of CYP19 aromatase activity in vitro.

    Science.gov (United States)

    Vinggaard, A M; Hnida, C; Breinholt, V; Larsen, J C

    2000-06-01

    Many pesticides are able to block or activate the steroid hormone receptors and/or to affect the levels of sex hormones, thereby potentially affecting the development or expression of the male and female reproductive system or both. This emphasizes the relevance of screening pesticides for a wide range of hormone-mimicking effects. Twenty-two pesticides were tested for their ability to affect CYP19 aromatase activity in human placental microsomes using the classical [(3)H](2)O method. Prochloraz, imazalil, propioconazole, fenarimol, triadimenol, triadimefon (all fungicides), and dicofol (an acaricide) gave rise to a statistically significant inhibition of aromatase activity. The IC(50)s of prochloraz, imazalil, propioconazole fenarimol, triadimenol, and triadimefon were calculated from dose-response curves to be 0.04, 0.34, 6.5, 10, 21 and 32 microM, respectively. The IC(50) of dicofol was greater than 50 microM. The positive control 4-hydroxyandrostendione (1 microM) caused an inhibition of aromatase activity by 74%. The compounds, which did not affect the aromatase activity, were bromopropylate, chlorfenvinphos, chlorobenzilate, chlorpyrifos, diuron, heptachlor, iprodion, linuron, pentachlorphenol, procymidon, propyzamide, quintozen, tetrachlorvinphos and tetradifon. With the purpose of comparing the results for fenarimol obtained with the microsomal system with data from an intact cell system, an aromatase assay based on JEG-3 cells was established. 4-Hydroxyandrostendione (1 microM) inhibited the aromatase activity in JEG-3 cells by 94%. The IC(50) for fenarimol in this system was 2 microM, slightly lower than that observed in the microsomal system. For the first time, fenarimol has been demonstrated to inhibit aromatase activity in human tissues and, furthermore, propioconazole, triadimefon, and triadimenol were identified as weak aromatase inhibitors. In conclusion, seven out of 22 tested pesticides turned out to be weak to moderate aromatase inhibitors in

  1. Phytochemical screening, cytotoxicity and antiviral activity of hexane fraction of Phaleria macrocarpa fruits

    Science.gov (United States)

    Ismaeel, Mahmud Yusef Yusef; Yaacob, Wan Ahmad; Tahir, Mariya Mohd.; Ibrahim, Nazlina

    2015-09-01

    Phaleria macrocarpa fruits have been widely used in the traditional medicine for the treatment of several infections. The current study was done to determine the phytochemical content, cytotoxicity and antiviral activity of the hexane fraction (HF) of P. macrocarpa fruits. In the hexane fraction of P. macarocarpa fruits, phytochemical screening showed the presence of terpenoids whereas saponins, alkaloids, tannins and anthraquinones were not present. Evaluation on Vero cell lines by using MTT assay showed that the 50% cytotoxic concentration (CC50) value was 0.48 mg/mL indicating that the fraction is not cytotoxic. Antiviral properties of the plant extracts were determined by plaque reduction assay. The effective concentration (EC50) was 0.18 mg/mL. Whereas the selective index (SI = CC50/EC50) of hexane fraction is 2.6 indicating low to moderate potential as antiviral agent.

  2. Phytochemical screening and Haemolytic activities of hydroalcoholic extract of Santalum album .L leaves

    Directory of Open Access Journals (Sweden)

    Deepak.TK

    2014-08-01

    Full Text Available The present study has been designed to screen the phytochemical constituents present in the hydroalcoholic extract of Santalum album linn leaves to ascertain the presence of saponins and futher studies carried out on the extract to evaluate its haemolytic activity towards bovine erythrocytes. Haemolytic effect of S. album leaf extract was evaluated according to the WHO guidelines in which the varying concentration of the extract was treated with the blood and lysis was determined visually. The result revealed that the S. album leaf extract produced lysis of erythrocyte at a minimum concentration of 475μg/ml. These observations will stimulate further research in the field of phytochemistry and also in clinical application of the phytochemical constituents of S. album. L.

  3. In vitro activity assays for MYST histone acetyltransferases and adaptation for high-throughput inhibitor screening

    Science.gov (United States)

    McCullough, Cheryl E.; Marmorstein, Ronen

    2016-01-01

    Lysine acetylation is a post-translational modification that is carried out by acetyltransferases. The MYST proteins form the largest and most diverse family of acetyltransferases, which regulate gene expression, DNA repair, and cell cycle homeostasis, among other activities, by acetylating both histone and non-histone proteins. This chapter will describe methods for the preparation and biochemical characterization of MYST family acetyltransferases, including protocols for the preparation of recombinant protein, enzyme assays for measuring steady state parameters and binding assays to measure cofactor and inhibitor binding. We also provide details on adapting these assays for high throughput screening for small molecule MYST inhibitors. This chapter seeks to prepare researchers for some hurdles that they may encounter when studying the MYST proteins so that there may be better opportunity to plan appropriate controls and obtain high quality data. PMID:27372752

  4. Screening of bacterial strains for pectinolytic activity: characterization of the polygalacturonase produced by Bacillus sp

    Directory of Open Access Journals (Sweden)

    Soares Márcia M.C.N.

    1999-01-01

    Full Text Available One hundred sixty eight bacterial strains, isolated from soil and samples of vegetable in decomposition, were screened for the use of citrus pectin as the sole carbon source. 102 were positive for pectinase depolymerization in assay plates as evidenced by clear hydrolization halos. Among them, 30% presented considerable pectinolytic activity. The cultivation of these strains by submerged and semi-solid fermentation for polygalacturonase production indicated that five strains of Bacillus sp produced high quantities of the enzyme. The physico-chemical characteristics, such as optimum pH of 6.0 - 7.0, optimum temperatures between 45oC and 55oC, stability at temperatures above 40oC and in neutral and alkaline pH, were determined.

  5. AMYLOLYTIC ACTIVITIES OF FUNGI SPECIES ON THE SCREENING MEDIUM ADJUSTED TO DIFFERENT pH

    OpenAIRE

    Balkan, Bilal; Aydoğdu, Halide; BALKAN, Seda; ERTAN, Figen

    2014-01-01

    The purpose of this study was to determine the amylolytic activities in different fungal species on the medium with different pH values. In the study, thirty-eight fungal species were screened by using a plate culture method on Czapek-Dox Agar medium with different pH values for the determination of amylase production. Among the tested fungal species; four species on medium adjusted to pH 4.0, ten species on medium with pH 4.5, nine species on medium with pH 5.0, four species on medium with p...

  6. Phytochemical Screening and Antibacterial Activity of Globimetulla browni Extracts During Wet Season

    Directory of Open Access Journals (Sweden)

    H.M. Inuwa

    2012-02-01

    Full Text Available The study investigated the phytochemical composition of Globimetulla browni for it’s ascribed folkloric medicinal uses as an antidiabetic and to establish its Antibacterial potency (if any. A comparative investigation was carried out and season did not have any effect on the phytochemical/Antibacterial potency of this plant. The ethanolic and aqueous extracts significantly affected both gram-negative and gram- positive microorganisms during wet season (May - September. Globimetulla browni is a specie of African mistletoe and is hemi-parasitic in nature growing on many trees e.g., Eukalyptus and has ascribed medicinal uses. Phytochemical screening showed the presence of carbohydrates, alkaloids, tannins and flavonoids. The ethanolic and aqueous extracts inhibited the growth of Klebsiella aerogenes, Proteus spp., Escherichia coli and Pseudomonas aeruginosa. Gentamycin and Cloxacillin did not exhibit any activity against Pseudomonas aeruginosa.

  7. Characterization and screening of antimicrobial activity of Micromonospora strains from Thai soils

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    Songsumanus, A.

    2013-01-01

    Full Text Available Aims: Rare actinomycete strains were isolated from mountain soils and island soil collected in Thailand. They were screened for antimicrobial activity and characterized for their secondary metabolites.Methodology and results: The strains were isolated by the standard dilution technique using starch casein nitrate agar. They were identified and characterized based on the phenotypic, chemotaxonomic and genotypic characteristics. The chemotaxonomic characteristics of ten isolates coincided with those of the genus Micromonospora. On the basis of phylogenetic analysis using 16S rRNA gene sequences and DNA-DNA relatedness, they were divided into 6 Groups, ASC19-2-1 (Group A was identified as Micromonospora marina; AL8-8 and AL10-3 (Group B were M. aurantiaca; AL7-5 (Group C was M. chalcea; AL3-16 and AL9-20 (Group D were identified as M. chokoriensis; AL9-13 and AL9-22 (Group E were M. tulbaghiae; and AL1-15-2 and AL1-16B (Group F were M. chersina. On the primary screening, only the isolate AL7-5 (Group C could inhibit Kocuria rhizophila ATCC 9341. This isolate produced rakicidin when cultivated on A3M, A11M and A16 media and produced compound BU4664L only on A16 medium.Conclusion, significance and impact of study: The isolation and characterization of the rare actinomycetes from Thai soils will be useful for the taxonomic study and for the discovery of bioactive metabolites that are active against microorganisms.

  8. Versatile assays for high throughput screening for activators or inhibitors of intracellular proteases and their cellular regulators.

    Directory of Open Access Journals (Sweden)

    Hideki Hayashi

    Full Text Available Intracellular proteases constitute a class of promising drug discovery targets. Methods for high throughput screening against these targets are generally limited to in vitro biochemical assays that can suffer many technical limitations, as well as failing to capture the biological context of proteases within the cellular pathways that lead to their activation. METHODS #ENTITYSTARTX00026;We describe here a versatile system for reconstituting protease activation networks in yeast and assaying the activity of these pathways using a cleavable transcription factor substrate in conjunction with reporter gene read-outs. The utility of these versatile assay components and their application for screening strategies was validated for all ten human Caspases, a family of intracellular proteases involved in cell death and inflammation, including implementation of assays for high throughput screening (HTS of chemical libraries and functional screening of cDNA libraries. The versatility of the technology was also demonstrated for human autophagins, cysteine proteases involved in autophagy.Altogether, the yeast-based systems described here for monitoring activity of ectopically expressed mammalian proteases provide a fascile platform for functional genomics and chemical library screening.

  9. In Vitro Biologic Activities of the Antimicrobials Triclocarban, Its Analogs, and Triclosan in Bioassay Screens: Receptor-Based Bioassay Screens

    OpenAIRE

    Ahn, Ki Chang; Zhao, Bin; Chen, Jiangang; Cherednichenko, Gennady; Sanmarti, Enio; Denison, Michael S.; Lasley, Bill; Pessah, Isaac N; Kültz, Dietmar; Chang, Daniel P.Y.; Gee, Shirley J.; Hammock, Bruce D.

    2008-01-01

    Background Concerns have been raised about the biological and toxicologic effects of the antimicrobials triclocarban (TCC) and triclosan (TCS) in personal care products. Few studies have evaluated their biological activities in mammalian cells to assess their potential for adverse effects. Objectives In this study, we assessed the activity of TCC, its analogs, and TCS in in vitro nuclear-receptor–responsive and calcium signaling bioassays. Materials and methods We determined the biological ac...

  10. In vitro biological screening of the anticholinesterase and antiproliferative activities of medicinal plants belonging to Annonaceae

    Directory of Open Access Journals (Sweden)

    A.S.N. Formagio

    2015-04-01

    Full Text Available The aim of this research was to investigate the antiproliferative and anticholinesterase activities of 11 extracts from 5 Annonaceae species in vitro. Antiproliferative activity was assessed using 10 human cancer cell lines. Thin-layer chromatography and a microplate assay were used to screen the extracts for acetylcholinesterase (AchE inhibitors using Ellman's reagent. The chemical compositions of the active extracts were investigated using high performance liquid chromatography. Eleven extracts obtained from five Annonaceae plant species were active and were particularly effective against the UA251, NCI-470 lung, HT-29, NCI/ADR, and K-562 cell lines with growth inhibition (GI50 values of 0.04-0.06, 0.02-0.50, 0.01-0.12, 0.10-0.27, and 0.02-0.04 µg/mL, respectively. In addition, the Annona crassiflora and A. coriacea seed extracts were the most active among the tested extracts and the most effective against the tumor cell lines, with GI50 values below 8.90 µg/mL. The A. cacans extract displayed the lowest activity. Based on the microplate assay, the percent AchE inhibition of the extracts ranged from 12 to 52%, and the A. coriacea seed extract resulted in the greatest inhibition (52%. Caffeic acid, sinapic acid, and rutin were present at higher concentrations in the A. crassiflora seed samples. The A. coriacea seeds contained ferulic and sinapic acid. Overall, the results indicated that A. crassiflora and A. coriacea extracts have antiproliferative and anticholinesterase properties, which opens up new possibilities for alternative pharmacotherapy drugs.

  11. In vitro biological screening of the anticholinesterase and antiproliferative activities of medicinal plants belonging to Annonaceae.

    Science.gov (United States)

    Formagio, A S N; Vieira, M C; Volobuff, C R F; Silva, M S; Matos, A I; Cardoso, C A L; Foglio, M A; Carvalho, J E

    2015-04-01

    The aim of this research was to investigate the antiproliferative and anticholinesterase activities of 11 extracts from 5 Annonaceae species in vitro. Antiproliferative activity was assessed using 10 human cancer cell lines. Thin-layer chromatography and a microplate assay were used to screen the extracts for acetylcholinesterase (AchE) inhibitors using Ellman's reagent. The chemical compositions of the active extracts were investigated using high performance liquid chromatography. Eleven extracts obtained from five Annonaceae plant species were active and were particularly effective against the UA251, NCI-470 lung, HT-29, NCI/ADR, and K-562 cell lines with growth inhibition (GI50) values of 0.04-0.06, 0.02-0.50, 0.01-0.12, 0.10-0.27, and 0.02-0.04 µg/mL, respectively. In addition, the Annona crassiflora and A. coriacea seed extracts were the most active among the tested extracts and the most effective against the tumor cell lines, with GI50 values below 8.90 µg/mL. The A. cacans extract displayed the lowest activity. Based on the microplate assay, the percent AchE inhibition of the extracts ranged from 12 to 52%, and the A. coriacea seed extract resulted in the greatest inhibition (52%). Caffeic acid, sinapic acid, and rutin were present at higher concentrations in the A. crassiflora seed samples. The A. coriacea seeds contained ferulic and sinapic acid. Overall, the results indicated that A. crassiflora and A. coriacea extracts have antiproliferative and anticholinesterase properties, which opens up new possibilities for alternative pharmacotherapy drugs.

  12. In vitro biological screening of the anticholinesterase and antiproliferative activities of medicinal plants belonging to Annonaceae

    Energy Technology Data Exchange (ETDEWEB)

    Formagio, A.S.N.; Vieira, M.C. [Faculdade de Ciências Agrárias, Universidade Federal da Grande Dourados, Dourados, MS (Brazil); Volobuff, C.R.F.; Silva, M.S. [Faculdade de Ciências Biológicas e Ambientais, Universidade Federal da Grande Dourados, Dourados, MS (Brazil); Matos, A.I. [Faculdade de Ciências, Universidade de Lisboa, Lisboa (Portugal); Cardoso, C.A.L. [Curso de Química, Universidade Estadual do Mato Grosso do Sul, Dourados, MS (Brazil); Foglio, M.A.; Carvalho, J.E. [Centro Pluridisciplinar de Pesquisas Químicas, Biológicas e Agrícolas, Universidade Estadual de Campinas, Campinas, SP (Brazil)

    2015-02-13

    The aim of this research was to investigate the antiproliferative and anticholinesterase activities of 11 extracts from 5 Annonaceae species in vitro. Antiproliferative activity was assessed using 10 human cancer cell lines. Thin-layer chromatography and a microplate assay were used to screen the extracts for acetylcholinesterase (AchE) inhibitors using Ellman's reagent. The chemical compositions of the active extracts were investigated using high performance liquid chromatography. Eleven extracts obtained from five Annonaceae plant species were active and were particularly effective against the UA251, NCI-470 lung, HT-29, NCI/ADR, and K-562 cell lines with growth inhibition (GI{sub 50}) values of 0.04-0.06, 0.02-0.50, 0.01-0.12, 0.10-0.27, and 0.02-0.04 µg/mL, respectively. In addition, the Annona crassiflora and A. coriacea seed extracts were the most active among the tested extracts and the most effective against the tumor cell lines, with GI{sub 50} values below 8.90 µg/mL. The A. cacans extract displayed the lowest activity. Based on the microplate assay, the percent AchE inhibition of the extracts ranged from 12 to 52%, and the A. coriacea seed extract resulted in the greatest inhibition (52%). Caffeic acid, sinapic acid, and rutin were present at higher concentrations in the A. crassiflora seed samples. The A. coriacea seeds contained ferulic and sinapic acid. Overall, the results indicated that A. crassiflora and A. coriacea extracts have antiproliferative and anticholinesterase properties, which opens up new possibilities for alternative pharmacotherapy drugs.

  13. Screening of Venezuelan medicinal plant extracts for cytostatic and cytotoxic activity against tumor cell lines.

    Science.gov (United States)

    Taylor, Peter; Arsenak, Miriam; Abad, María Jesús; Fernández, Angel; Milano, Balentina; Gonto, Reina; Ruiz, Marie-Christine; Fraile, Silvia; Taylor, Sofía; Estrada, Omar; Michelangeli, Fabian

    2013-04-01

    There are estimated to be more than 20,000 species of plants in Venezuela, of which more than 1500 are used for medicinal purposes by indigenous and local communities. Only a relatively small proportion of these have been evaluated in terms of their potential as antitumor agents. In this study, we screened 308 extracts from 102 species for cytostatic and cytotoxic activity against a panel of six tumor cell lines using a 24-h sulphorhodamine B assay. Extracts from Clavija lancifolia, Hamelia patens, Piper san-vicentense, Physalis cordata, Jacaranda copaia, Heliotropium indicum, and Annona squamosa were the most cytotoxic, whereas other extracts from Calotropis gigantea, Hyptis dilatata, Chromolaena odorata, Siparuna guianensis, Jacaranda obtusifolia, Tapirira guianensis, Xylopia aromatica, Protium heptaphyllum, and Piper arboreum showed the greatest cytostatic activity. These results confirm previous reports on the cytotoxic activities of the above-mentioned plants as well as prompting further studies on others such as C. lancifolia and H. dilatata that have not been so extensively studied. PMID:22648665

  14. Screening of Bacterial Strains for Polygalacturonase Activity: Its Production by Bacillus sphaericus (MTCC 7542

    Directory of Open Access Journals (Sweden)

    Ranveer Singh Jayani

    2010-01-01

    Full Text Available At present almost all the pectinolytic enzymes used for industrial applications are produced by fungi. There are a few reports of pectinase production by bacterial strains. Therefore, in the present study, seventy-four bacterial strains, isolated from soil and rotten vegetable samples, were screened for polygalacturonase production. The strain PG-31, which gave maximum activity, was identified as Bacillus sphaericus (MTCC 7542. Maximal quantities of polygalacturonase were produced when a 16-hours-old inoculum was used at 7.5% (v/v in production medium and incubated in shaking conditions (160 rpm for 72 hours. The optimal temperature and pH for bacterial growth and polygalacturonase production were found to be 30∘C and 6.8, respectively. Maximum enzyme production resulted when citrus pectin was used as the carbon source at a concentration of 1.25% (w/v, whereas other carbon sources led to a decrease (30%–70% in enzyme production. Casein hydrolysate and yeast extract used together as organic nitrogen source gave best results, and ammonium chloride was found to be the most suitable inorganic nitrogen source. The supplementation of media with 0.9% (w/v D-galacturonic acid led to a 23% increase in activity. Bacillus sphaericus, a bacterium isolated from soil, produced good amount of polygalacturonase activity at neutral pH; hence, it would be potentially useful to increase the yield of banana, grape, or apple juice.

  15. Synthesis, Characterization, Antimicrobial Screening and Free-Radical Scavenging Activity of Some Novel Substituted Pyrazoles

    Directory of Open Access Journals (Sweden)

    Nagwa Mohamed Mahrous Hamada

    2015-06-01

    Full Text Available The present work deals with the synthesis of acetoxysulfonamide pyrazole derivatives, substituted 4,5-dihydropyrazole-1-carbothioamide and 4,5-dihydropyrazole-1-isonicotinoyl derivatives starting from substituted vanillin chalcones. Acetoxysulfonamide pyrazole derivatives were prepared from the reaction of chalcones with p-sulfamylphenylhydrazine followed by treatment with acetic anhydride. At the same time 4,5-dihydropyrazole-1-carbothioamide and 4,5-dihydropyrazole-1-isonicotinoyl derivatives were prepared from the reaction of chalcones with either thiosemicarbazide or isonicotinic acid hydrazide, respectively. The synthesized compounds were structurally characterized on the basis of IR, 1H-NMR, 13C-NMR spectral data and microanalyses. All of the newly isolated compounds were tested for their antimicrobial activities. The antimicrobial screening using the agar well-diffusion method revealed that the chloro derivatives are the most active ones. Moreover, the antioxidant and anti-inflammatory activity of these chloro derivatives are also studied using the DPPH radical scavenging and NO radical scavenging methods, respectively.

  16. Screening of selected ethnomedicinal plants from South Africa for larvicidal activity against the mosquito Anopheles arabiensis

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    Maharaj Rajendra

    2012-09-01

    Full Text Available Abstract Background This study was initiated to establish whether any South African ethnomedicinal plants (indigenous or exotic, that have been reported to be used traditionally to repel or kill mosquitoes, exhibit effective mosquito larvicidal properties. Methods Extracts of a selection of plant taxa sourced in South Africa were tested for larvicidal properties in an applicable assay. Thirty 3rd instar Anopheles arabiensis larvae were exposed to various extract types (dichloromethane, dichloromethane/methanol (1:1, methanol and purified water of each species investigated. Mortality was evaluated relative to the positive control Temephos (Mostop; Agrivo, an effective emulsifiable concentrate larvicide. Results Preliminary screening of crude extracts revealed substantial variation in toxicity with 24 of the 381 samples displaying 100% larval mortality within the seven day exposure period. Four of the high activity plants were selected and subjected to bioassay guided fractionation. The results of the testing of the fractions generated identified one fraction of the plant, Toddalia asiatica as being very potent against the An. arabiensis larvae. Conclusion The present study has successfully identified a plant with superior larvicidal activity at both the crude and semi pure fractions generated through bio-assay guided fractionation. These results have initiated further research into isolating the active compound and developing a malaria vector control tool.

  17. Assessment of Antimalarial Activity against Plasmodium falciparum and Phytochemical Screening of Some Yemeni Medicinal Plants

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    Mohammed A. Alshawsh

    2009-01-01

    Full Text Available Developing countries, where malaria is one of the most prevalent diseases, still rely on traditional medicine as a source for the treatment of this disease. In the present study, six selected plants (Acalypha fruticosa, Azadirachta indica, Cissus rotundifolia, Echium rauwalfii, Dendrosicyos socotrana and Boswellia elongata commonly used in Yemen by traditional healers for the treatment of malaria as well as other diseases, were collected from different localities of Yemen, dried and extracted with methanol and water successfully. The antiplasmodial activity of the extracts was evaluated against fresh clinical isolates of Plasmodium falciparum. The selectivity parameters to evaluate the efficacy of these medicinal plants were measured by in vitro micro test (Mark III according to World Health Organization (WHO 1996 & WHO 2001 protocols of antimalarial drug tests. Among the investigated 12 extracts, three were found to have significant antiplasmodial activity with IC50 values less than 4 µg/ml, namely the water extracts of A. fruticosa, A. indica and D. socotrana. Six extracts showed moderate activity with IC50 values ranging from 10 to 30 µg/ml and three appeared to be inactive with IC50 values more than 30 µg/ml. In addition, preliminary phytochemical screening of the methanolic and aqueous extracts indicated the presence of saponins, tannins, flavonoids, terpenoids, polysaccharides and peptides.

  18. Profiling Physical Activity, Diet, Screen and Sleep Habits in Portuguese Children

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    Sara Pereira

    2015-06-01

    Full Text Available Obesity in children is partly due to unhealthy lifestyle behaviours, e.g., sedentary activity and poor dietary choices. This trend has been seen globally. To determine the extent of these behaviours in a Portuguese population of children, 686 children 9.5 to 10.5 years of age were studied. Our aims were to: (1 describe profiles of children’s lifestyle behaviours; (2 identify behaviour pattern classes; and (3 estimate combined effects of individual/ socio-demographic characteristics in predicting class membership. Physical activity and sleep time were estimated by 24-h accelerometry. Nutritional habits, screen time and socio-demographics were obtained. Latent Class Analysis was used to determine unhealthy lifestyle behaviours. Logistic regression analysis predicted class membership. About 78% of children had three or more unhealthy lifestyle behaviours, while 0.2% presented no risk. Two classes were identified: Class 1-Sedentary, poorer diet quality; and Class 2-Insufficiently active, better diet quality, 35% and 65% of the population, respectively. More mature children (Odds Ratio (OR = 6.75; 95%CI = 4.74–10.41, and boys (OR = 3.06; 95% CI = 1.98–4.72 were more likely to be overweight/obese. However, those belonging to Class 2 were less likely to be overweight/obese (OR = 0.60; 95% CI = 0.43–0.84. Maternal education level and household income did not significantly predict weight status (p ≥ 0.05.

  19. Screening of lactic acid bacteria from vacuum packaged beef for antimicrobial activity

    Science.gov (United States)

    Oliveira, Roseane B. P.; de L. Oliveira, Afonso; Glória, M. Beatriz A.

    2008-01-01

    The objective of this study was to isolate lactic acid bacteria (LAB) from vacuum packaged beef and to investigate their antagonist activity. LAB mean counts of 5.19 log cfu/cm2 were obtained from five samples of vacuum packaged beef. Two hundred isolates were selected and screened for the inhibitory effect on five ATCC reference Lactobacillus strains. Thirty six isolates showed activity in the agar spot test against at least two of the indicator strains. However, only six cell free supernatants (CFS) from these isolates exhibited activity against the indicator strains using the well-diffusion test and conditions that eliminated the effects of organic acids and hydrogen peroxide. L. acidophilus was the most sensitive indicator tested, whereas L. plantarum and L. fermentum were the most resistant ones. Identification by MIDI system indicated that these LAB isolates were Lactococcus lactis subsp. cremoris, Pediococcus acidilactici, Lactobacillus delbrueckii subsp. bulgaricus and Lactobacillus casei GC subgroup A. The antagonistic factors produced by most of these LAB against L. acidophilus were resistant to heat treatment (100°C for 10 min) and stable over a wide pH range (4.0 to 9.0). These data suggest that these isolates could be used as promising hurdles aiming increased safety and extended shelf life of meat products. PMID:24031232

  20. Screening of Venezuelan medicinal plant extracts for cytostatic and cytotoxic activity against tumor cell lines.

    Science.gov (United States)

    Taylor, Peter; Arsenak, Miriam; Abad, María Jesús; Fernández, Angel; Milano, Balentina; Gonto, Reina; Ruiz, Marie-Christine; Fraile, Silvia; Taylor, Sofía; Estrada, Omar; Michelangeli, Fabian

    2013-04-01

    There are estimated to be more than 20,000 species of plants in Venezuela, of which more than 1500 are used for medicinal purposes by indigenous and local communities. Only a relatively small proportion of these have been evaluated in terms of their potential as antitumor agents. In this study, we screened 308 extracts from 102 species for cytostatic and cytotoxic activity against a panel of six tumor cell lines using a 24-h sulphorhodamine B assay. Extracts from Clavija lancifolia, Hamelia patens, Piper san-vicentense, Physalis cordata, Jacaranda copaia, Heliotropium indicum, and Annona squamosa were the most cytotoxic, whereas other extracts from Calotropis gigantea, Hyptis dilatata, Chromolaena odorata, Siparuna guianensis, Jacaranda obtusifolia, Tapirira guianensis, Xylopia aromatica, Protium heptaphyllum, and Piper arboreum showed the greatest cytostatic activity. These results confirm previous reports on the cytotoxic activities of the above-mentioned plants as well as prompting further studies on others such as C. lancifolia and H. dilatata that have not been so extensively studied.

  1. PHYTOCHEMICAL SCREENING, FLAVONOID CONTENT AND ANTIOXIDANT ACTIVITY OF ETHANOLIC EXTRACT OF CEIBA PENTANDRA

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    Talole Bhagyashri

    2013-02-01

    Full Text Available The seed of Ceiba pentandra collected from the rural area of Shirur, Pune district, were dried, milled and extracted with ether, ethanol and water. Phytochemical screening was carried out according to standard procedures. Carbohydrate & flavonoids, fixed oil, glycosides were found to be present in the aqueous, ether & alcoholic extract resp. Total Flavonoid content was determined by spectrophotometric methods and that was found to be 2.56 g & 2.20g quercetin equivalent per 100 g of ethanolic & water extract resp. In-vitro antioxidant activity of ethanolic seed extract of Ceiba pentandra was determined by DPPH free radical scavanging assay. All the analysis was made with the use of UV-Visible Spectrophotometer (Jasco V-530. The ethanolic seed extracts of Ceiba pentandra had shown very significant DPPH (1, 1-diphenyl-2-picryl-hydrazyl radical scavenging activity compared to standard antioxidant. The DPPH radical scavenging activity of the extract was increased with the increasing concentration. In DPPH free radical scavanging assay IC50 value of ethanolic seed extracts of Ceiba pentandra was found to be 50.33±5.29 as compared with standard ascorbic acid (44.93±2.92 µg/ml.

  2. Antibiotic pigment from desert soil actinomycetes; biological activity, purification and chemical screening

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    Selvameenal L

    2009-01-01

    Full Text Available An actinomycete strain, Streptomyces hygroscopicus subsp. ossamyceticus (strain D10 was isolated from Thar Desert soil, Rajasthan during the year 2006 and found to produce a yellow color pigment with antibiotic activity. Crude pigment was produced from strain D10 by solid state fermentation using wheat bran medium followed by extraction with ethyl acetate. The antimicrobial activity of the crude pigment was evaluated against drug resistant pathogens such as methicillin-resistant Staphylococcus aureus, vancomycin-resistant Staphylococcus aureus, extended spectrum b-lactamase producing cultures of Escherichia coli, Pseudomonas aeruginosa and Klebsiella sp. About 420 mg of crude pigment was produced per 10 g of wheat bran medium. In the disc diffusion method the crude ethyl acetate extract showed a minimum of 10 mm inhibition against Klebsiella sp. and maximum of 19 mm of inhibition against Escherichia coli. The crude pigment was partially purified using thin layer chromatography with the solvent system chloroform:methanol (30:70 and the Rf value was calculated as 0.768. Antimicrobial activity of the partially purified compound from thin layer chromatography was determined using the bioautography method. The purified pigment showed minimum of 15 mm inhibition against Klebsiella sp. and a maximum of 23 mm of inhibition against vancomycin-resistant Staphylococcus aureus in the disc diffusion method. Based on the results of chemical screening, the pigment was tentatively identified as group of sugar containing molecules.

  3. A Novel High-Throughput 3D Screening System for EMT Inhibitors: A Pilot Screening Discovered the EMT Inhibitory Activity of CDK2 Inhibitor SU9516

    Science.gov (United States)

    Eguchi, Takanori; Rahman, M. Mamunur; Sakamoto, Ruriko; Masuda, Norio; Nakatsura, Tetsuya; Calderwood, Stuart K.; Kozaki, Ken-ichi; Itoh, Manabu

    2016-01-01

    Epithelial-mesenchymal transition (EMT) is a crucial pathological event in cancer, particularly in tumor cell budding and metastasis. Therefore, control of EMT can represent a novel therapeutic strategy in cancer. Here, we introduce an innovative three-dimensional (3D) high-throughput screening (HTS) system that leads to an identification of EMT inhibitors. For the establishment of the novel 3D-HTS system, we chose NanoCulture Plates (NCP) that provided a gel-free micro-patterned scaffold for cells and were independent of other spheroid formation systems using soft-agar. In the NCP-based 3D cell culture system, A549 lung cancer cells migrated, gathered, and then formed multiple spheroids within 7 days. Live cell imaging experiments showed that an established EMT-inducer TGF-β promoted peripheral cells around the core of spheroids to acquire mesenchymal spindle shapes, loss of intercellular adhesion, and migration from the spheroids. Along with such morphological change, EMT-related gene expression signatures were altered, particularly alteration of mRNA levels of ECAD/CDH1, NCAD/CDH2, VIM and ZEB1/TCF8. These EMT-related phenotypic changes were blocked by SB431542, a TGF-βreceptor I (TGFβR1) inhibitor. Inside of the spheroids were highly hypoxic; in contrast, spheroid-derived peripheral migrating cells were normoxic, revealed by visualization and quantification using Hypoxia Probe. Thus, TGF-β-triggered EMT caused spheroid hypoplasia and loss of hypoxia. Spheroid EMT inhibitory (SEMTIN) activity of SB431542 was calculated from fluorescence intensities of the Hypoxia Probe, and then was utilized in a drug screening of EMT-inhibitory small molecule compounds. In a pilot screening, 9 of 1,330 compounds were above the thresholds of the SEMTIN activity and cell viability. Finally, two compounds SB-525334 and SU9516 showed SEMTIN activities in a dose dependent manner. SB-525334 was a known TGFβR1 inhibitor. SU9516 was a cyclin-dependent kinase 2 (CDK2) inhibitor

  4. A Novel High-Throughput 3D Screening System for EMT Inhibitors: A Pilot Screening Discovered the EMT Inhibitory Activity of CDK2 Inhibitor SU9516.

    Science.gov (United States)

    Arai, Kazuya; Eguchi, Takanori; Rahman, M Mamunur; Sakamoto, Ruriko; Masuda, Norio; Nakatsura, Tetsuya; Calderwood, Stuart K; Kozaki, Ken-Ichi; Itoh, Manabu

    2016-01-01

    Epithelial-mesenchymal transition (EMT) is a crucial pathological event in cancer, particularly in tumor cell budding and metastasis. Therefore, control of EMT can represent a novel therapeutic strategy in cancer. Here, we introduce an innovative three-dimensional (3D) high-throughput screening (HTS) system that leads to an identification of EMT inhibitors. For the establishment of the novel 3D-HTS system, we chose NanoCulture Plates (NCP) that provided a gel-free micro-patterned scaffold for cells and were independent of other spheroid formation systems using soft-agar. In the NCP-based 3D cell culture system, A549 lung cancer cells migrated, gathered, and then formed multiple spheroids within 7 days. Live cell imaging experiments showed that an established EMT-inducer TGF-β promoted peripheral cells around the core of spheroids to acquire mesenchymal spindle shapes, loss of intercellular adhesion, and migration from the spheroids. Along with such morphological change, EMT-related gene expression signatures were altered, particularly alteration of mRNA levels of ECAD/CDH1, NCAD/CDH2, VIM and ZEB1/TCF8. These EMT-related phenotypic changes were blocked by SB431542, a TGF-βreceptor I (TGFβR1) inhibitor. Inside of the spheroids were highly hypoxic; in contrast, spheroid-derived peripheral migrating cells were normoxic, revealed by visualization and quantification using Hypoxia Probe. Thus, TGF-β-triggered EMT caused spheroid hypoplasia and loss of hypoxia. Spheroid EMT inhibitory (SEMTIN) activity of SB431542 was calculated from fluorescence intensities of the Hypoxia Probe, and then was utilized in a drug screening of EMT-inhibitory small molecule compounds. In a pilot screening, 9 of 1,330 compounds were above the thresholds of the SEMTIN activity and cell viability. Finally, two compounds SB-525334 and SU9516 showed SEMTIN activities in a dose dependent manner. SB-525334 was a known TGFβR1 inhibitor. SU9516 was a cyclin-dependent kinase 2 (CDK2) inhibitor

  5. Phytochemical screening and free radical scavenging activity of Citrullus colocynthis seeds extracts

    Institute of Scientific and Technical Information of China (English)

    Nabila; Benariba; Rabeh; Djaziri; Wafaa; Bellakhdar; Nacera; Belkacem; Marcel; Kadiata; Willy; J.Malaisse; Abdullah; Sener

    2013-01-01

    Objective:To study the phytochemical screening of different extracts from Citrullus colocynthis(C.colocynthis)seeds extracts and to assess their antioxidant activity on the DPPH free radical scavenging.Methods:Phytochemical screening,total content of polyphenols and flavonoids of C.colocynthis seeds extracts,including a crude aqueous extract(E1),a defatted aqueous extract(E2),a hydromethanolic extract(HM),an ethyl acetate extract(EA)and a n-butanol extract(n-B)was carried out according to the standard methods and to assess their corresponding effect on the antioxidant activity of this plant.Results:None of these extracts contained detectable amount of alkaloid,quinone,antraquinone,or reducing sugar.Catechic tannins and flavonoids were abundant in E1,MM and EA,whilst terpenoids were abundantly present in E1 and n-B but only weekly in HM.Coumarins were found in E2,EA and n-B.Polyphenols,expressed as gallic acid equivalent,amounted,per 100 g plant matter,to 329,1002 and 150 mg in EA,HM an E1 respectively.Flavonoids,expressed as catechin equivalent,amounted.per 100 g plant matter to 620,241 and 94 mg in EA,HM and E1 respectively.Comparable values were found in n-B and E1,with lower values in E2.Quercetin,myricetin and gallic acid were found in the EA and HM extracts by thin layer chromatography,The antioxidative effect of these extracts yielded,when tested at a concentration of 2000μg/mL in a 1,1-diphenyl-2-picrylhydrazyl assay,a reducing percentage of 88.8%with EA,74.5%with HM and 66.2%with E1,and corresponding IC50of 350,580and 500μg/mL as compared to 1.1μg/mL for ascorbic acid.Conclusions:These qualitative and quantitative analytical data document the presence in C.colocynthis extracts of such chemical compounds as flavonoids responsible for the antioxidant activity,as well as other biological activities of this plant.

  6. Phytochemical screening and free radical scavenging activity of Citrullus colocynthis seeds extracts

    Institute of Scientific and Technical Information of China (English)

    Nabila Benariba; Rabeh Djaziri; Wafaa Bellakhdar; Nacera Belkacem; Marcel Kadiata; Willy J Malaisse; Abdullah Sener

    2013-01-01

    Objective: To study the phytochemical screening of different extracts from Citrullus colocynthis (C. colocynthis ) seeds extracts and to assess their antioxidant activity on the DPPH free radical scavenging. Methods: Phytochemical screening, total content of polyphenols and flavonoids ofC. colocynthis seeds extracts, including a crude aqueous extract (E1), a defatted aqueous extract (E2), a hydromethanolic extract (HM), an ethyl acetate extract (EA) and a n-butanol extract (n-B) was carried out according to the standard methods and to assess their corresponding effect on the antioxidant activity of this plant. Results: None of these extracts contained detectable amount of alkaloid, quinone, antraquinone, or reducing sugar. Catechic tannins and flavonoids were abundant in E1, HM and EA, whilst terpenoids were abundantly present in E1 and n-B but only weekly in HM. Coumarins were found in E2, EA and n-B. Polyphenols, expressed as gallic acid equivalent, amounted, per 100 g plant matter, to 329, 1002 and 150 mg in EA, HM an E1 respectively. Flavonoids, expressed as catechin equivalent, amounted, per 100 g plant matter to 620, 241 and 94 mg in EA, HM and E1 respectively. Comparable values were found in n-B and E1, with lower values in E2. Quercetin, myricetin and gallic acid were found in the EA and HM extracts by thin layer chromatography, The antioxidative effect of these extracts yielded, when tested at a concentration of 2000 μg/mL in a 1,1-diphenyl-2-picrylhydrazyl assay, a reducing percentage of 88.8% with EA, 74.5% with HM and 66.2% with E1, and corresponding IC50 of 350, 580 and 500 μg/mL as compared to 1.1 μg/mL for ascorbic acid. Conclusions: These qualitative and quantitative analytical data document the presence in C. colocynthis extracts of such chemical compounds as flavonoids responsible for the antioxidant activity, as well as other biological activities of this plant.

  7. Development and Implementation of a Smartphone Application to Promote Physical Activity and Reduce Screen-Time in Adolescent Boys

    OpenAIRE

    Lubans, David R; Smith, Jordan J.; Skinner, Geoff; Morgan, Philip J

    2014-01-01

    Purpose: To describe the development and implementation of a smartphone application (app) designed to promote physical activity and reduce screen-time in adolescent boys considered “at-risk” of obesity. Methods: An app was developed to support the delivery of a face-to-face school-based obesity prevention program known as the “Active Teen Leaders Avoiding Screen-time” (ATLAS) program. ATLAS was guided by self-determination theory and social cognitive theory and evaluated using a cluster ra...

  8. Development and Implementation of a Smartphone Application to Promote Physical Activity and Reduce Screen-time in Adolescent Boys

    OpenAIRE

    David Revalds Lubans; Jordan eSmith; Geoff eSkinner; Philip James Morgan

    2014-01-01

    Purpose: The primary aim is to describe the development and implementation of a smartphone application (app) designed to promote physical activity and reduce screen-time in adolescent boys ‘at risk’ of obesity from low-income communities.Methods: An app was developed to support the delivery of a face-to-face school-based obesity prevention program known as the ‘Active Teen Leaders Avoiding Screen-time’ (ATLAS) program. ATLAS was guided by self-determination theory and social cognitive theory ...

  9. Children′s physical activity and screen time: qualitative comparison of views of parents of infants and preschool children

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    Hesketh Kylie D

    2012-12-01

    Full Text Available Abstract Background While parents are central to the development of behaviours in their young children, little is known about how parents view their role in shaping physical activity and screen time behaviours. Methods Using an unstructured focus group design, parental views and practices around children′s physical activity and screen time (television and computer use were explored with eight groups of new parents (n=61; child age Results Parents generally believed children are naturally active, which may preclude their engagement in strategies designed to increase physical activity. While parents across both age groups shared many overarching views concerning parenting for children′s physical activity and screen time behaviours, some strategies and barriers differed depending on the age of the child. While most new parents were optimistic about their ability to positively influence their child′s behaviours, many parents of preschool-aged children seemed more resigned to strategies that worked for them, even when aware such strategies may not be ideal. Conclusions Interventions aiming to increase children′s physical activity and decrease screen time may need to tailor strategies to the age group of the child and address parents′ misconceptions and barriers to optimum parenting in these domains.

  10. Phytochemical screening and antioxidant, antimitotic, and antiproliferative activities of Trichodesma indicum shoot

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    Shweta S Saboo

    2014-01-01

    Full Text Available Background: Traditionally Trichodesma indicum has been used for its therapeutic effect in folk medicine that include anti-inflammatory, analgesic and anticancer properties. In this work, we validate the anticancer potential of the plant. Aims: To screen the shoot extracts T. indicum for their antimitotic and antiproliferative activities. Materials and Methods: The dried aerial parts of T. indicum were successively extracted with petroleum ether, successive chloroform extract (SCH, successive ethanol extract (SEE and water. The plant extracts were subjected to study of in vitro antioxidant activity using 2,2′- diphenyl-1-picrylhydrazyl, 2,2′- azino-bis(3-ethylbenzothiazoline-6-sulphonic acid radical inhibition systems. The extracts were also tested for their in vitro antimitotic activity in Allium cepa root and antiproliferative activity using the yeast model and five human cell lines (MCF-7, HOP-62, MOLT-4, HCT-15 and PRO. Result and Conclusion: The mitotic index for SCH and SEE was found to be 12.01 ± 1.34 and 12.99 ± 0.25 mg/mL, respectively. The IC 50 value in the antiproliferative assay was found to be 30.14-35.36 mg/mL for SCH and SEE respectively. Both SCH and SEE extracts showed significant antimitotic and antiproliferative activity when compared to the standard methothreaxate, vincreastine and adriamycin. Among the extracts, SEE showed strong inhibition against MCF-7 and MOLT-4 cell lines at concentration <30 μg/mL. Phytochemical analysis of extracts indicated the presence of β-sitosterol, gallic acid and catechin. Based on these results, it is concluded that T. indicum may be a good candidate for the treatment of a variety of cancer. Thus, its traditional use is validated.

  11. Phytochemicals Screening and Activities of Hydrophilic and Lipophilic Antioxidant of Some Fruit Peels

    International Nuclear Information System (INIS)

    This study was conducted to screen the secondary metabolites compounds including alkaloids, tannins, saponins and flavonoids as well as to determine the antioxidant activities of four types of fruit peels namely Psidium guajava (guava), Mangifera indica (Chakonan mango), Citrus sinensis (Navel orange) and Malus sylvestris (Granny Smith apple). The hydrophilic and lipophilic antioxidant activities were investigated using three different assays such as Ferric Reducing Antioxidant Power (FRAP), 2, 2-diphenyl-1-picrylhydrazyl (DPPH) scavenging activity and Oxygen Radical Absorbance Capacity (ORAC). Total Phenolic Content (TPC) and Total Flavonoids Content (TFC) were also conducted and the correlations between the antioxidant assays with TPC and TFC were evaluated. The TPC in the peels extract ranged between 204.90 to 517.00 mg GAE/ g extract weight while TFC ranged between 97.48 to 177.86 mg QE/ g extract weight. The FRAP, EC50 scavenging activity and ORAC values were 18.78 to 45.36 mM TE/ 100 g extract weight, 0.146 to 0.717 mg/ ml scavenging effect and 37.54 to 60.59 μM TE/ g extract weight respectively. The extract of M. indica peels appeared to be as potent as ascorbic acid with maximum inhibition of 74 % at 200 ppm. M. indica peels showed highest value in all antioxidant assays and in TPC while the highest in TFC was found in M. sylvestris peels. There were strong correlations between all antioxidant assays with TPC but very weak correlations with TFC. This study suggested that the extracts of fruit peels are convenient to be use as functional ingredients in food product development as they are rich in antioxidant activities. (author)

  12. Terrestrial actinomycetes from diverse locations of Uttarakhnad, India: Isolation and screening for their antibacterial activity.

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    Vijay Kumar

    2013-09-01

    Full Text Available Uttarakhand region is less explored, but possess a great biodiversity. This diversity can be explored for isolation and characterization of new actinomycetes strains for seeking antimicrobial molecules. It can therefore be predicted that novel bioactive metabolite producing actinomycetes can be discovered to combat multidrug resistant bacterial pathogens.Variations in the viable count of actinomycetes were accessed in different altitudes. Actinomycetes were isolated, indentified and screened for their antibacterial activity.The highest viable counts of actinomycetes were recorded in valleys followed by mid hills and high hills. A total of 512 actinomycetes were isolated which were found to belong the 14 different genera of actinomycetes. Mainly the genus Streptomyces was dominant in all the soil samples. Out of 512 isolates recovered, 23.44% exhibited antibacterial activity against one or more tested bacterial pathogens. Of these 56.67% showed activity against Gram-positive bacteria, 26.67% against Gram-negative bacteria while 16.67% showed broad spectrum activity. Isolate DV1S and GR9a-5 showed highest antibacterial properties against several multi-drug resistant bacterial pathogens and were identified using polyphasic approach. DV1S and GR9a-5 were found to be most closely related with S. massasporeus NBRC 12796(T and Nocardia nova JCM 6044(T respectively.The results of this study strongly support the idea that the viable count of actinomycetes varied greatly with altitude. The actinomycetes species isolated from valleys, mid hills and high hills possess significant capacity to produce compounds which are active against several drug resistant bacterial pathogens.

  13. Transposon activation mutagenesis as a screening tool for identifying resistance to cancer therapeutics

    International Nuclear Information System (INIS)

    The development of resistance to chemotherapies represents a significant barrier to successful cancer treatment. Resistance mechanisms are complex, can involve diverse and often unexpected cellular processes, and can vary with both the underlying genetic lesion and the origin or type of tumor. For these reasons developing experimental strategies that could be used to understand, identify and predict mechanisms of resistance in different malignant cells would be a major advance. Here we describe a gain-of-function forward genetic approach for identifying mechanisms of resistance. This approach uses a modified piggyBac transposon to generate libraries of mutagenized cells, each containing transposon insertions that randomly activate nearby gene expression. Genes of interest are identified using next-gen high-throughput sequencing and barcode multiplexing is used to reduce experimental cost. Using this approach we successfully identify genes involved in paclitaxel resistance in a variety of cancer cell lines, including the multidrug transporter ABCB1, a previously identified major paclitaxel resistance gene. Analysis of co-occurring transposons integration sites in single cell clone allows for the identification of genes that might act cooperatively to produce drug resistance a level of information not accessible using RNAi or ORF expression screening approaches. We have developed a powerful pipeline to systematically discover drug resistance in mammalian cells in vitro. This cost-effective approach can be readily applied to different cell lines, to identify canonical or context specific resistance mechanisms. Its ability to probe complex genetic context and non-coding genomic elements as well as cooperative resistance events makes it a good complement to RNAi or ORF expression based screens

  14. Recent Advances in Screening of Anti-Campylobacter Activity in Probiotics for Use in Poultry.

    Science.gov (United States)

    Saint-Cyr, Manuel J; Guyard-Nicodème, Muriel; Messaoudi, Soumaya; Chemaly, Marianne; Cappelier, Jean-Michel; Dousset, Xavier; Haddad, Nabila

    2016-01-01

    Campylobacteriosis is the most common cause of bacterial gastroenteritis worldwide. Campylobacter species involved in this infection usually include the thermotolerant species Campylobacter jejuni. The major reservoir for C. jejuni leading to human infections is commercial broiler chickens. Poultry flocks are frequently colonized by C. jejuni without any apparent symptoms. Risk assessment analyses have identified the handling and consumption of poultry meat as one of the most important sources of human campylobacteriosis, so elimination of Campylobacter in the poultry reservoir is a crucial step in the control of this foodborne infection. To date, the use of probiotics has demonstrated promising results to reduce Campylobacter colonization. This review provides recent insights into methods used for probiotic screening to reduce the prevalence and colonization of Campylobacter at the farm level. Different eukaryotic epithelial cell lines are employed to screen probiotics with an anti-Campylobacter activity and yield useful information about the inhibition mechanism involved. These in vitro virulence models involve only human intestinal or cervical cell lines whereas the use of avian cell lines could be a preliminary step to investigate mechanisms of C. jejuni colonization in poultry in the presence of probiotics. In addition, in vivo trials to evaluate the effect of probiotics on Campylobacter colonization are conducted, taking into account the complexity introduced by the host, the feed, and the microbiota. However, the heterogeneity of the protocols used and the short time duration of the experiments lead to results that are difficult to compare and draw conclusions at the slaughter-age of broilers. Nevertheless, the combined approach using complementary in vitro and in vivo tools (cell cultures and animal experiments) leads to a better characterization of probiotic strains and could be employed to assess reduced Campylobacter spp. colonization in chickens if some

  15. Recent Advances in Screening of Anti-Campylobacter Activity in Probiotics for Use in Poultry

    Science.gov (United States)

    Saint-Cyr, Manuel J.; Guyard-Nicodème, Muriel; Messaoudi, Soumaya; Chemaly, Marianne; Cappelier, Jean-Michel; Dousset, Xavier; Haddad, Nabila

    2016-01-01

    Campylobacteriosis is the most common cause of bacterial gastroenteritis worldwide. Campylobacter species involved in this infection usually include the thermotolerant species Campylobacter jejuni. The major reservoir for C. jejuni leading to human infections is commercial broiler chickens. Poultry flocks are frequently colonized by C. jejuni without any apparent symptoms. Risk assessment analyses have identified the handling and consumption of poultry meat as one of the most important sources of human campylobacteriosis, so elimination of Campylobacter in the poultry reservoir is a crucial step in the control of this foodborne infection. To date, the use of probiotics has demonstrated promising results to reduce Campylobacter colonization. This review provides recent insights into methods used for probiotic screening to reduce the prevalence and colonization of Campylobacter at the farm level. Different eukaryotic epithelial cell lines are employed to screen probiotics with an anti-Campylobacter activity and yield useful information about the inhibition mechanism involved. These in vitro virulence models involve only human intestinal or cervical cell lines whereas the use of avian cell lines could be a preliminary step to investigate mechanisms of C. jejuni colonization in poultry in the presence of probiotics. In addition, in vivo trials to evaluate the effect of probiotics on Campylobacter colonization are conducted, taking into account the complexity introduced by the host, the feed, and the microbiota. However, the heterogeneity of the protocols used and the short time duration of the experiments lead to results that are difficult to compare and draw conclusions at the slaughter-age of broilers. Nevertheless, the combined approach using complementary in vitro and in vivo tools (cell cultures and animal experiments) leads to a better characterization of probiotic strains and could be employed to assess reduced Campylobacter spp. colonization in chickens if some

  16. 儿童慢性骨髓炎应用抗感染活性骨Ⅰ期植骨治疗的疗效评价%Evaluation of the therapeutic effects of anti-infective reconstituted bone xenograft on chronic osteomyelitis in children

    Institute of Scientific and Technical Information of China (English)

    袁志; 刘建; 胡蕴玉; 刘建敏; 黄鲁豫; 李丹; 孟国林; 毕龙

    2009-01-01

    Objective To study the effect of anti-infective reconstituted bone xenograft (ARBX) as one-stage grafting on treating various chronic osteomyelitis in children. Methods ARBX was used to treat 16 cases of various chronic osteomyelitis in children as one-stage grafting after debridement since September of 2001. There were 8 cases with haematogenous, 3 with primary and 5 with traumatic chronic osteomyelitis. All patients were followed up for an average period of 39 months (range, 12 to 79 months). Results Except 1 case got recurrent infection and another 1 with nonunion due to large segmental bone defect after operation, other 14 cases were cured with the cure rate was 87. 5% (14/16), which is higher than that of classical therapy. Conclusions ARBX has high osteoinductive activity and enhanced anti-infective capability, which enables it to be used as one-stage grafting to treat various chronic osteomyelitis in children.%目的 验证抗感染活性骨(anti-infective reconstituted bone xenograft,ARBX)Ⅰ期植骨治疗儿童慢性骨髓炎的疗效.方法 自2001年9月对21例慢性骨髓炎患儿进行病灶清除,应用抗感染活性异种骨(anti-infective reconstituted bone xenograft,ARBX)Ⅰ期植骨治疗,其中获得12个月以上随访的儿童慢性骨髓炎患儿共16例.包括血源性慢性骨髓炎8例,原发性慢性骨髓炎3例,创伤性慢性骨髓炎5例.结果 16例中除1例骨髓炎复发,1例骨髓炎合并大段骨缺损在术后发生骨不连外,其余14例感染均获得控制无复发,病变部位均获得确实骨修复.本组感染治愈率(感染控制且无复发)为93.8%,完全治愈率(感染控制既无复发又完成骨修复)为87.5%.结论 ARBX具有高效诱导成骨活性和强效抗感染能力,是Ⅰ期植骨治疗儿童慢性骨髓炎的有效方法.

  17. Maternal and paternal parenting practices and their influence on children's adiposity, screen-time, diet and physical activity.

    Science.gov (United States)

    Lloyd, Adam B; Lubans, David R; Plotnikoff, Ronald C; Collins, Clare E; Morgan, Philip J

    2014-08-01

    The primary aim of this study was to examine a range of potential behavioral and maternal/paternal correlates of adiposity in children. Secondary aims were to examine (a) correlates of screen-time, diet and physical activity and (b) if there were differences in maternal and paternal physical activity- and dietary-related parenting practices. Cross-sectional analysis was conducted using 70 families with children (59% boys (41/70), mean age 8.4 (±2.4) years). Parenting practices were measured using the Parenting Strategies for Eating and Activity Scale. Children's outcomes included: 7-day pedometry (physical activity), screen-time, percent energy from core foods (Food frequency questionnaire) and BMI z-score. Multiple regression models were generated to examine the associations between maternal and paternal parenting practices and children's variables. In the regression analyses, fathers' BMI (p parenting practices [limit setting (p = .01), reinforcement (p = .02)] and child screen-time (p = .02) were significantly associated with intake of core foods. Despite some similarities within families, three out of five parenting constructs were significantly different between mothers and fathers. Mothers and fathers have different parental influences on their children's weight status and lifestyle behaviors and both should be included in lifestyle interventions targeting children. A focus on maternal parenting specifically relating to screen-time and diet, and father's physical activity parenting and weight status may support their children in developing more healthy behaviors.

  18. Screening Physical Activity in Family Practice: Validity of the Spanish Version of a Brief Physical Activity Questionnaire.

    Directory of Open Access Journals (Sweden)

    Anna Puig-Ribera

    Full Text Available The use of brief screening tools to identify inactive patients is essential to improve the efficiency of primary care-based physical activity (PA programs. However, the current employment of short PA questionnaires within the Spanish primary care pathway is unclear. This study evaluated the validity of the Spanish version of a Brief Physical Activity Assessment Tool (SBPAAT.A validation study was carried out within the EVIDENT project. A convenience sample of patients (n = 1,184; age 58.9±13.7 years; 60.5% female completed the SBPAAT and the 7-day Physical Activity Recall (7DPAR and, in addition, wore an accelerometer (ActiGraph GT3X for seven consecutive days. Validity was evaluated by measuring agreement, Kappa correlation coefficients, sensitivity and specificity in achieving current PA recommendations with the 7DPAR. Pearson correlation coefficients with the number of daily minutes engaged in moderate and vigorous intensity PA according to the accelerometer were also assessed. Comparison with accelerometer counts, daily minutes engaged in sedentary, light, moderate, and vigorous intensity PA, total daily kilocalories, and total PA and leisure time expenditure (METs-hour-week between the sufficiently and insufficiently active groups identified by SBPAAT were reported.The SBPAAT identified 41.3% sufficiently active (n = 489 and 58.7% insufficiently active (n = 695 patients; it showed moderate validity (k = 0.454, 95% CI: 0.402-0.505 and a specificity and sensitivity of 74.3% and 74.6%, respectively. Validity was fair for identifying daily minutes engaged in moderate (r = 0.215, 95% CI:0.156 to 0.272 and vigorous PA (r = 0.282, 95% CI:0.165 to 0.391. Insufficiently active patients according to the SBPAAT significantly reported fewer counts/minute (-22%, fewer minutes/day of moderate (-11.38 and vigorous PA (-2.69, spent fewer total kilocalories/day (-753, and reported a lower energy cost (METs-hour-week of physical activities globally (-26

  19. Screening of radical scavenging activity and polyphenol content of Bulgarian plant species

    Directory of Open Access Journals (Sweden)

    Milena Nikolova

    2011-01-01

    Full Text Available Background: Discovery of new plant species with antioxidant properties is a priority of many research teams. Most of the species included in this study are unstudied for antioxidant properties, but they are taxonomically related to reference plants with well-documented antioxidant activity. Materials and Methods: Free radical scavenging activity of plant extracts was evaluated using a 1,1-diphenyl-2-picrylhydrazyl (DPPH assay. An aluminum chloride colorimetric method was used for flavonoid determination. The amount of phenolic compounds in the extracts was estimated by using the Folin-Ciocalteu reagent. Results: As a result of screening, it was found that the significant antioxidant properties possess several unstudied until now plant species (Veronica bellidioides L., V. kellereri Deg. et Urm, V. vindobonensis (M. Fisher M. Fisher, V. beccabunga L., V. rhodopaea L., V. austriaca (Velen. Degen., Clinopodium vulgare L., Stachys recta L., Clematis vitalba L., and Xeranthemum annum L.. The antioxidant potential of the new species is comparable to that of reference medicinal plants. Conclusions: The existing data presented here provide new information for antioxidant potential of plant species that have not been traditionally used as medicinal plants.

  20. PHYTOCHEMICAL SCREENING AND MICROBICIDAL ACTIVITY OF STEM BARK OF PTEROCARPUS MARSUPIUM

    Directory of Open Access Journals (Sweden)

    Udaysing Hari Patil,

    2011-01-01

    Full Text Available Bactericidal potential of methanolic extract of stem bark (Apical bark, middle bark and Mature bark of Pterocarpus marsupium was evaluated with respect to pathogenic bacteria Bacillus subtilis, Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoneae, Salmonella typhi, Proteus mirabilis and Micrococcus sp. The methanolic extract of apical stem bark was effective than the middle bark and mature bark in inhibiting the growth of all bacteria. The bacterium Staphylococcus aureus was most sensitive among all the bacterial species studied. Preliminary phytochemical analysis revealed the presence of alkaloids, glycosides,flavonoids, flavonols, phenols and terpenoids. Saponins were absent in all the bark samples.The concentrations of these phytoconstituents was higher in the apical stem bark than the middle and mature stem bark. The percent extract yield was maximum in apical stem bark. Thus, in the pharmacological point of view, it is important to study the biochemistry of apical bark in order to isolate and screen the new pharmacological active principals which can be useful in designing of new drugs active against various infectious micro- rganisms like bacteria, fungi and viruses etc.

  1. Discovery of New Compounds Active against Plasmodium falciparum by High Throughput Screening of Microbial Natural Products

    Science.gov (United States)

    Pérez-Moreno, Guiomar; Cantizani, Juan; Sánchez-Carrasco, Paula; Ruiz-Pérez, Luis Miguel; Martín, Jesús; el Aouad, Noureddine; Pérez-Victoria, Ignacio; Tormo, José Rubén; González-Menendez, Víctor; González, Ignacio; de Pedro, Nuria; Reyes, Fernando; Genilloud, Olga; Vicente, Francisca; González-Pacanowska, Dolores

    2016-01-01

    Due to the low structural diversity within the set of antimalarial drugs currently available in the clinic and the increasing number of cases of resistance, there is an urgent need to find new compounds with novel modes of action to treat the disease. Microbial natural products are characterized by their large diversity provided in terms of the chemical complexity of the compounds and the novelty of structures. Microbial natural products extracts have been underexplored in the search for new antiparasitic drugs and even more so in the discovery of new antimalarials. Our objective was to find new druggable natural products with antimalarial properties from the MEDINA natural products collection, one of the largest natural product libraries harboring more than 130,000 microbial extracts. In this work, we describe the optimization process and the results of a phenotypic high throughput screen (HTS) based on measurements of Plasmodium lactate dehydrogenase. A subset of more than 20,000 extracts from the MEDINA microbial products collection has been explored, leading to the discovery of 3 new compounds with antimalarial activity. In addition, we report on the novel antiplasmodial activity of 4 previously described natural products. PMID:26735308

  2. Physical activity reduces risk for colon polyps in a multiethnic colorectal cancer screening population

    Directory of Open Access Journals (Sweden)

    Sanchez Nelson F

    2012-06-01

    Full Text Available Abstract Background Identifying modifiable factors that influence the epidemiology of colorectal cancer incidence among multiethnic groups might be informative for the development of public health strategies targeting the disease. Minimal data exists describing the impact of physical activity on colorectal polyp risk in United States minority populations. The aim of this study is to evaluate the relationship of exercise on the prevalence of polyps in a multiethnic colorectal cancer screening population. Results We enrolled 982 patients: 558 Hispanic, 202 Asian,149 Black, and 69 White. Patients who reported exercising one or more hours weekly had a lower prevalence of any polyps (25.3% vs 33.2%, P = 0.008 as well as adenomas (13.8 vs. 18.9%, P = 0.03 compared to those who did not exercise. Black and Hispanic patients and those who were overweight or obese also had lower prevalence of polyps if they led an active lifestyle. Multivariate analysis revealed that age >55, male sex, and Black race/ethnicity were positively associated with the presence of adenomas, while a history of exercising one hour or more weekly was an independent negative predictor for the presence of adenomas anywhere in the colon (OR 0.67; 95% CI 0.4 - 0.9, P = 0.03. Conclusions Exercising one hour per week was associated with a lower prevalence of polyps and adenomas when compared to those who exercised less or not at all. An active lifestyle provides benefits to groups who are at risk for colorectal cancer, such as Blacks. It also provides significant protection to overweight and obese individuals. Public health initiatives should promote physical activity as a cancer prevention tool in multiethnic populations. Trial registration none

  3. β2-Adrenoceptor affinity chromatography and its application in the screening of the active compounds from Semen Armeniacae Amarum

    Institute of Scientific and Technical Information of China (English)

    ZHENG XiaoHui; ZHAO XinFeng; YANG Rong; WANG ShiXiang; WEI YinMao; ZHENG JianBin

    2008-01-01

    β2-Adrenoceptor (β2-AR) was purified from the rabbit lung tissue by sepharose-salbutamol affinity chromatographic column. To prepare the β2-AR stationary phase, β2-AR was evenly immobilized on the surface of macro-pore silica with a mild chemical coupling method through covalent bond. The reten-tion properties of β2-AR stationary phase were characterized by four ligands, salbutamol sulfate, noradrenaline bitartrate, adrenaline hydrochloride and propranolol hydrochloride, to establish the β2-AR affinity chromatography. Then, the method was used to screen the active compounds from the total extracts of Semen Armeniacae Amarum. The results showed that β2-AR on the surface of the sta-tionary phase could keep its original bioactivity and selectivity. Amygdalin retained in the chroma-tographic column was proved to be the active compound of the total extracts of Semen Armeniacae Amarum. Compared with the existing chromatographic screening approaches, this method showed a good stability and high selectivity. The active compounds which could interact with β2-AR in traditional Chinese medicine (TCM) could be screened efficiently by this method, providing a new way to screen the active compounds in complicated samples such as TCM.

  4. Screen time, adiposity and cardiometabolic markers : mediation by physical activity, not snacking, among 11-year-old children

    NARCIS (Netherlands)

    Berentzen, N. E.; Smit, H. A.; van Rossem, L.; Gehring, U.; Kerkhof, M.; Postma, D. S.; Boshuizen, H. C.; Wijga, A. H.

    2014-01-01

    BACKGROUND: There is evidence for a relation of TV viewing with adiposity and increased cardiometabolic risk factors in children and adolescents. It is unclear to what extent this relation is mediated by snacking and lack of physical activity. We determined whether associations of screen time with a

  5. Screen time, adiposity and cardiometabolic markers: mediation by physical activity, not snacking, among 11-year-old children

    NARCIS (Netherlands)

    Berendtzen, N.E.; Smit, H.A.; Rossem, van L.; Gehring, U.; Kerkhof, van de M.; Postma, D.S.; Boshuizen, H.C.

    2014-01-01

    Background:There is evidence for a relation of TV viewing with adiposity and increased cardiometabolic risk factors in children and adolescents. It is unclear to what extent this relation is mediated by snacking and lack of physical activity. We determined whether associations of screen time with ad

  6. Phytochemical screening, free radical scavenging, antioxidant activity and phenolic content of Dodonaea viscosa

    Directory of Open Access Journals (Sweden)

    Riaz Tauheeda

    2012-01-01

    Full Text Available The purpose of this study was to evaluate the antioxidant potential of Dodonaea viscosa Jacq. Methanolic extract of the plant was dissolved in distilled water and partitioned with n-hexane, chloroform, ethyl acetate and nbutanol sequentially. Phytochemical screening showed presence of phenolics, flavonoides and cardiac glycosides in large amount in chloroform, ethyl acetate and n-butanol fraction. The antioxidant potential of all these fractions and remaining aqueous fraction was evaluated by four methods: 1,1-Diphenyl-2-picrylhydrazyl (DPPH free radical scavenging activity, total antioxidant activity, Ferric Reducing Antioxidant Power (FRAP assay and ferric thiocyanate assay along with determination of their total phenolics. The results revealed that ethyl acetate soluble fraction exhibited highest percent inhibition of DPPH radical as compared to other fractions. It showed 81.14 ± 1.38% inhibition of DPPH radical at a concentration of 60 μg/ml. The IC50 of this fraction was found to be 33.95 ± 0.58 μg/ml, relative to butylated hydroxytoluene (BHT, having IC50 of 12.54 ± 0.89 μg/mL. It also showed highest FRAP value (380.53 ± 0.74 μM of trolox equivalents as well as highest total phenolic contents (208.58 ± 1.83 GAE μg/g and highest value of inhibition of lipid peroxidation (58.11 ± 1.49% at concentration of 500 μg/ml as compared to the other studied fractions. The chloroform fraction showed highest total antioxidant activity i.e.1.078 ± 0.59 (eq. to BHT.

  7. Discovery of small molecule inhibitors of xyloglucan endotransglucosylase (XET) activity by high-throughput screening

    Science.gov (United States)

    Chormova, Dimitra; Franková, Lenka; Defries, Andrew; Cutler, Sean R.; Fry, Stephen C.

    2015-01-01

    Small molecules (xenobiotics) that inhibit cell-wall-localised enzymes are valuable for elucidating the enzymes’ biological roles. We applied a high-throughput fluorescent dot-blot screen to search for inhibitors of Petroselinum xyloglucan endotransglucosylase (XET) activity in vitro. Of 4216 xenobiotics tested, with cellulose-bound xyloglucan as donor-substrate, 18 inhibited XET activity and 18 promoted it (especially anthraquinones and flavonoids). No compounds promoted XET in quantitative assays with (cellulose-free) soluble xyloglucan as substrate, suggesting that promotion was dependent on enzyme–cellulose interactions. With cellulose-free xyloglucan as substrate, we found 22 XET-inhibitors – especially compounds that generate singlet oxygen (1O2) e.g., riboflavin (IC50 29 μM), retinoic acid, eosin (IC50 27 μM) and erythrosin (IC50 36 μM). The riboflavin effect was light-dependent, supporting 1O2 involvement. Other inhibitors included tannins, sulphydryl reagents and triphenylmethanes. Some inhibitors (vulpinic acid and brilliant blue G) were relatively specific to XET, affecting only two or three, respectively, of nine other wall-enzyme activities tested; others [e.g. (−)-epigallocatechin gallate and riboflavin] were non-specific. In vivo, out of eight XET-inhibitors bioassayed, erythrosin (1 μM) inhibited cell expansion in Rosa and Zea cell-suspension cultures, and 40 μM mycophenolic acid and (−)-epigallocatechin gallate inhibited Zea culture growth. Our work showcases a general high-throughput strategy for discovering wall-enzyme inhibitors, some being plant growth inhibitors potentially valuable as physiological tools or herbicide leads. PMID:26093490

  8. Phytochemical screening, antioxidant and cytotoxic activity of fruit extracts of Calamus tenuis Roxb

    Institute of Scientific and Technical Information of China (English)

    Zaki Uddin Ahmed; Seheli Sejuti Bithi; Md Minhazur Rahman Khan; Md Mofazzol Hossain; Suriya Sharmin; Satyajit Roy Rony

    2014-01-01

    Objective:To investigate the antioxidant and cytotoxic activity of the fruits of Calamus tenuis Roxb. Methods:The preliminary phytochemical group tests were done, which revealed the presence of alkaloid, tannin, flavonoid and steroid. The dried fruit was extracted in soxhlet apparatus using petroleum ether, ethyl acetate and methanol. Antioxidant potential of each extract was evaluated using total phenol content, total flavonoid content, cupric reducing antioxidant capacity, 1,1-diphenyl-2-picrylhydrazyl radical scavenging activity, and total antioxidant capacity determinations. Results:The extracts were found to possess moderate to high amounts of phenolic and flavonoid contents. In cupric reducing antioxidant capacity assay the extracts showed moderate reducing power which increases with concentration. Scavenging of 1,1-diphenyl-2-picrylhydrazyl radical was found to rise with concentration with lowest IC50 value for methanol extract, which was confirmed by total antioxidant activity test that shows highest (95 mg/g of extract) in ascorbic acid equivalent for methanol extract. In Brine shrimp lethality bioassay the methanol and petroleum ether extracts were found to be toxic to Brine shrimp nauplii, with LC50 of 25.53 µg/mL and 28.07 µg/mL respectively while the LC50 of the reference vincristine sulphate was 1.32 µg/mL. Ethyl acetate extract was found to be moderately cytotoxic showing LC50 of 47.79 µg/mL. Conclusions: The results of the present study suggest that the fruits of Calamus tenuis Roxb possess antioxidant and cytotoxic potential. Moreover, phytochemical screening reveals the presence of alkaloid, tannin, flavonoid and steroid, which may be responsible for the observed bioactivities.

  9. ROS-activated ATM-dependent phosphorylation of cytoplasmic substrates identified by large scale phosphoproteomics screen

    DEFF Research Database (Denmark)

    Kozlov, Sergei V; Waardenberg, Ashley J; Engholm-Keller, Kasper;

    2016-01-01

    substrates (HMGA1 and UIMCI/RAP80), another five were identified in a whole cell extract phosphoproteomic screens and the remaining four proteins had not been identified previously in DNA damage response screens. We validated the phosphorylation of three of these proteins (OSR1, HDGF and ccdc82) as ATM...

  10. Application of a cocktail approach to screen cytochrome P450 BM3 libraries for metabolic activity and diversity.

    Science.gov (United States)

    Reinen, Jelle; Postma, Geert; Tump, Cornelis; Bloemberg, Tom; Engel, Jasper; Vermeulen, Nico P E; Commandeur, Jan N M; Honing, Maarten

    2016-02-01

    In the present study, the validity of using a cocktail screening method in combination with a chemometrical data mining approach to evaluate metabolic activity and diversity of drug-metabolizing bacterial Cytochrome P450 (CYP) BM3 mutants was investigated. In addition, the concept of utilizing an in-house-developed library of CYP BM3 mutants as a unique biocatalytic synthetic tool to support medicinal chemistry was evaluated. Metabolic efficiency of the mutant library towards a selection of CYP model substrates, being amitriptyline (AMI), buspirone (BUS), coumarine (COU), dextromethorphan (DEX), diclofenac (DIC) and norethisterone (NET), was investigated. First, metabolic activity of a selection of CYP BM3 mutants was screened against AMI and BUS. Subsequently, for a single CYP BM3 mutant, the effect of co-administration of multiple drugs on the metabolic activity and diversity towards AMI and BUS was investigated. Finally, a cocktail of AMI, BUS, COU, DEX, DIC and NET was screened against the whole in-house CYP BM3 library. Different validated quantitative and qualitative (U)HPLC-MS/MS-based analytical methods were applied to screen for substrate depletion and targeted product formation, followed by a more in-depth screen for metabolic diversity. A chemometrical approach was used to mine all data to search for unique metabolic properties of the mutants and allow classification of the mutants. The latter would open the possibility of obtaining a more in-depth mechanistic understanding of the metabolites. The presented method is the first MS-based method to screen CYP BM3 mutant libraries for diversity in combination with a chemometrical approach to interpret results and visualize differences between the tested mutants. PMID:26753974

  11. Application of a cocktail approach to screen cytochrome P450 BM3 libraries for metabolic activity and diversity.

    Science.gov (United States)

    Reinen, Jelle; Postma, Geert; Tump, Cornelis; Bloemberg, Tom; Engel, Jasper; Vermeulen, Nico P E; Commandeur, Jan N M; Honing, Maarten

    2016-02-01

    In the present study, the validity of using a cocktail screening method in combination with a chemometrical data mining approach to evaluate metabolic activity and diversity of drug-metabolizing bacterial Cytochrome P450 (CYP) BM3 mutants was investigated. In addition, the concept of utilizing an in-house-developed library of CYP BM3 mutants as a unique biocatalytic synthetic tool to support medicinal chemistry was evaluated. Metabolic efficiency of the mutant library towards a selection of CYP model substrates, being amitriptyline (AMI), buspirone (BUS), coumarine (COU), dextromethorphan (DEX), diclofenac (DIC) and norethisterone (NET), was investigated. First, metabolic activity of a selection of CYP BM3 mutants was screened against AMI and BUS. Subsequently, for a single CYP BM3 mutant, the effect of co-administration of multiple drugs on the metabolic activity and diversity towards AMI and BUS was investigated. Finally, a cocktail of AMI, BUS, COU, DEX, DIC and NET was screened against the whole in-house CYP BM3 library. Different validated quantitative and qualitative (U)HPLC-MS/MS-based analytical methods were applied to screen for substrate depletion and targeted product formation, followed by a more in-depth screen for metabolic diversity. A chemometrical approach was used to mine all data to search for unique metabolic properties of the mutants and allow classification of the mutants. The latter would open the possibility of obtaining a more in-depth mechanistic understanding of the metabolites. The presented method is the first MS-based method to screen CYP BM3 mutant libraries for diversity in combination with a chemometrical approach to interpret results and visualize differences between the tested mutants.

  12. Sepsis Caused by Extended-Spectrum Beta-Lactamase (ESBL)-Positive K. pneumoniae and E. coli: Comparison of Severity of Sepsis, Delay of Anti-Infective Therapy and ESBL Genotype

    Science.gov (United States)

    Steinmetz, Ivo; Kohler, Christian; Pfeifer, Yvonne; Gastmeier, Petra; Schwab, Frank; Kola, Axel; Deja, Maria; Leistner, Rasmus

    2016-01-01

    Infections with extended-spectrum beta-lactamase-producing Enterobacteriaceae (ESBL-E) are associated with increased mortality. Outcome differences due to various species of ESBL-E or ESBL genotypes are not well investigated. We conducted a cohort study to assess risk factors for mortality in cases of ESBL-E bacteremia (K. pneumoniae or E. coli) and the risk factors for sepsis with organ failure. All consecutive patients of our institution from 2008 to 2011 with bacteremia due to ESBL-E were included. Basic epidemiological data, underlying comorbidities, origin of bacteremia, severity of sepsis and delay of appropriate anti-infective treatment were collected. Isolates were PCR-screened for the presence of ESBL genes and plasmid-mediated AmpC β-lactamases. Cox proportional hazard regression on mortality and multivariable logistic regression on risk factors for sepsis with organ failure was conducted. 219 cases were included in the analysis: 73.1% due to E. coli, 26.9% due to K. pneumoniae. There was no significant difference in hospital mortality (ESBL-E. coli, 23.8% vs. ESBL-K. pneumoniae 27.1%, p = 0.724). However, the risk of sepsis with organ failure was associated in cases of K. pneumoniae bacteremia (OR 4.5, p<0.001) and patients with liver disease (OR 3.4, p = 0.004) or renal disease (OR 6.8, p<0.001). We found significant differences in clinical presentation of ESBL-E bacteremia due to K. pneumoniae compared to E. coli. As K. pneumoniae cases showed a more serious clinical presentation as E. coli cases and were associated with different risk factors, treatment and prevention strategies should be adjusted accordingly. PMID:27442425

  13. Phytochemical screening and antioxidant activity of ethanol extract of Tithonia diversifolia(Hemsl)A.Gray dry flowers

    Institute of Scientific and Technical Information of China (English)

    Robson; Miranda; da; Gama; Marcelo; Guimares; Luiz; Carlos; de; Abreu; José; Armando-Junior

    2014-01-01

    Objective:To evaluate the antioxidant activity of extracts of dried flowers of Tithonia diversifolia(Hemsl) A.Gray(T.diversifolia) dry flower-a slirubby plant belonging to the Asteraceac family and very common in Brazil,providing data to help prevent premature aging skin.Methods:The tests of phytochemical screening included total phenols,tannins,flavonoids,alkaloids and saponins.The active antioxidant was determined by 2,2-diphenyl-1-picrylhydrazyl method.Results:The phytoehemical screening of T.diversifolia dry flowers revealed the presence of phenolic compounds(tannins,flavonoids and total phenolsi,while alkaloids and saponins were not detected.The IC50 values showed a strong antioxidant activity of the plant extracts.Conclusions:Therefore,this study suggests the possibility of using dry flowers extracts of T.diversifolia for the prevention of cell aging,as was shown to have significant antioxidant activity.

  14. A Simple Assay to Screen Antimicrobial Compounds Potentiating the Activity of Current Antibiotics

    Science.gov (United States)

    Iqbal, Junaid; Kazmi, Shahana Urooj; Khan, Naveed Ahmed

    2013-01-01

    Antibiotic resistance continues to pose a significant problem in the management of bacterial infections, despite advances in antimicrobial chemotherapy and supportive care. Here, we suggest a simple, inexpensive, and easy-to-perform assay to screen antimicrobial compounds from natural products or synthetic chemical libraries for their potential to work in tandem with the available antibiotics against multiple drug-resistant bacteria. The aqueous extract of Juglans regia tree bark was tested against representative multiple drug-resistant bacteria in the aforementioned assay to determine whether it potentiates the activity of selected antibiotics. The aqueous extract of J. regia bark was added to Mueller-Hinton agar, followed by a lawn of multiple drug-resistant bacteria, Salmonella typhi or enteropathogenic E. coli. Next, filter paper discs impregnated with different classes of antibiotics were placed on the agar surface. Bacteria incubated with extract or antibiotics alone were used as controls. The results showed a significant increase (>30%) in the zone of inhibition around the aztreonam, cefuroxime, and ampicillin discs compared with bacteria incubated with the antibiotics/extract alone. In conclusion, our assay is able to detect either synergistic or additive action of J. regia extract against multiple drug-resistant bacteria when tested with a range of antibiotics. PMID:23865073

  15. A Simple Assay to Screen Antimicrobial Compounds Potentiating the Activity of Current Antibiotics

    Directory of Open Access Journals (Sweden)

    Junaid Iqbal

    2013-01-01

    Full Text Available Antibiotic resistance continues to pose a significant problem in the management of bacterial infections, despite advances in antimicrobial chemotherapy and supportive care. Here, we suggest a simple, inexpensive, and easy-to-perform assay to screen antimicrobial compounds from natural products or synthetic chemical libraries for their potential to work in tandem with the available antibiotics against multiple drug-resistant bacteria. The aqueous extract of Juglans regia tree bark was tested against representative multiple drug-resistant bacteria in the aforementioned assay to determine whether it potentiates the activity of selected antibiotics. The aqueous extract of J. regia bark was added to Mueller-Hinton agar, followed by a lawn of multiple drug-resistant bacteria, Salmonella typhi or enteropathogenic E. coli. Next, filter paper discs impregnated with different classes of antibiotics were placed on the agar surface. Bacteria incubated with extract or antibiotics alone were used as controls. The results showed a significant increase (>30% in the zone of inhibition around the aztreonam, cefuroxime, and ampicillin discs compared with bacteria incubated with the antibiotics/extract alone. In conclusion, our assay is able to detect either synergistic or additive action of J. regia extract against multiple drug-resistant bacteria when tested with a range of antibiotics.

  16. Screening of plants acting against Heterometrus laoticus scorpion venom activity on fibroblast cell lysis.

    Science.gov (United States)

    Uawonggul, Nunthawun; Chaveerach, Arunrat; Thammasirirak, Sompong; Arkaravichien, Tarinee; Chuachan, Chattong; Daduang, Sakda

    2006-01-16

    The aqueous extracts of 64 plant species, listed as animal- or insect-bite antidotes in old Thai drug recipes were screened for their activity against fibroblast cell lysis after Heterometrus laoticus scorpion venom treatment. The venom was preincubated with plant extract for 30 min and furthered treated to confluent fibroblast cells for 30 min. More than 40% efficiency (test/control) was obtained from cell treatment with venom preincubated with extracts of Andrographis paniculata Nees (Acanthaceae), Barringtonia acutangula (L.) Gaertn. (Lecythidaceae), Calamus sp. (Palmae), Clinacanthus nutans Lindau (Acanthaceae), Euphorbia neriifolia L. (Euphorbiaceae), Ipomoea aquatica Forssk (Convolvulaceae), Mesua ferrea L. (Guttiferae), Passiflora laurifolia L. (Passifloraceae), Plectranthus amboinicus (Lour.) Spreng. (Labiatae), Ricinus communis L. (Euphorbiaceae), Rumex sp. (Polygonaceae) and Sapindus rarak DC. (Sapindaceae), indicating that they had a tendency to be scorpion venom antidotes. However, only Andrographis paniculata and Barringtonia acutangula extracts provided around 50% viable cells from extract treatments without venom preincubation. These two plant extracts are expected to be scorpion venom antidotes with low cytotoxicity. PMID:16169172

  17. Screening of immunomodulatory and adhesive Lactobacillus with antagonistic activities against Salmonella from fermented vegetables.

    Science.gov (United States)

    Feng, Junchang; Liu, Pilong; Yang, Xin; Zhao, Xin

    2015-12-01

    The purpose of this study was to select strains of lactic acid bacteria (LAB) by their in vitro adhesive and immunomodulatory properties for potential use as probiotics. In this study, 16 randomly selected LAB strains from fermented vegetables (sauerkraut, bean and cabbage) were first screened for their tolerance to acid, bile salts, pepsin and pancreatin, bacterial inhibitory activities and abilities to adherence to Caco-2 cells. Then, 4 strains with the highest adhesion abilities were selected for further studies of their immunomodulatory properties and inhibitory effects against Salmonella adhesion and invasion to Caco-2 cells in vitro. The results showed that these 16 LAB strains effectively survived in simulated gastrointestinal condition and inhibited growth of six tested pathogens. Lactobacillus rhamnosus P1, Lactobacillus plantarum P2, Lactobacillus rhamnosus P3 and Lactobacillus casei P4 had the highest abilities to adhere to Caco-2 cells. Furthermore, L. plantarum P2 strain showed higher abilities to induce expression of tumor necrosis factor-α and interleukin-12 by splenic monocytes and strongly inhibited the adhesion and invasion of S. enteritidis ATCC13076 to Caco-2 cells. These results suggest that Lactobacillus strains P2 could be used as a probiotic candidate in food against Salmonella infection.

  18. Screening of plant extracts for antimicrobial activity against bacteria and yeasts with dermatological relevance.

    Science.gov (United States)

    Weckesser, S; Engel, K; Simon-Haarhaus, B; Wittmer, A; Pelz, K; Schempp, C M

    2007-08-01

    There is cumulative resistance against antibiotics of many bacteria. Therefore, the development of new antiseptics and antimicrobial agents for the treatment of skin infections is of increasing interest. We have screened six plant extracts and isolated compounds for antimicrobial effects on bacteria and yeasts with dermatological relevance. The following plant extracts have been tested: Gentiana lutea, Harpagophytum procumbens, Boswellia serrata (dry extracts), Usnea barbata, Rosmarinus officinalis and Salvia officinalis (supercritical carbon dioxide [CO2] extracts). Additionally, the following characteristic plant substances were tested: usnic acid, carnosol, carnosic acid, ursolic acid, oleanolic acid, harpagoside, boswellic acid and gentiopicroside. The extracts and compounds were tested against 29 aerobic and anaerobic bacteria and yeasts in the agar dilution test. U. barbata-extract and usnic acid were the most active compounds, especially in anaerobic bacteria. Usnea CO2-extract effectively inhibited the growth of several Gram-positive bacteria like Staphylococcus aureus (including methicillin-resistant strains - MRSA), Propionibacterium acnes and Corynebacterium species. Growth of the dimorphic yeast Malassezia furfur was also inhibited by Usnea-extract. Besides the Usnea-extract, Rosmarinus-, Salvia-, Boswellia- and Harpagophytum-extracts proved to be effective against a panel of bacteria. It is concluded that due to their antimicrobial effects some of the plant extracts may be used for the topical treatment of skin disorders like acne vulgaris and seborrhoic eczema. PMID:17291738

  19. Preliminary Phytochemical Screening And Evaluation of Free Radical Scavenging Activity Of Stevia rebaudiana Bertoni From Different Geographical Sources

    OpenAIRE

    Bitasta Mandal; Swati Madan

    2013-01-01

    Stevia rebaudiana Bertoni, a natural non-caloric substitute to conventional sugar, is also popular as the “sweet herb of Paraguay”. It is a storehouse of various bioactive constituents mainly, the ent-kaurene diterpene glycosides namely stevioside, rebaudioside A, B, C, D and E. The plant is known to exhibit a wide range of biological activities like hypoglycemic, anti-oxidant, anticancer, antibacterial activities. The present research is based on a preliminary phytochemical screening and com...

  20. Screening breeding sites of the common toad (Bufo bufo) in England and Wales for evidence of endocrine disrupting activity.

    Science.gov (United States)

    Pickford, Daniel B; Jones, Alexandra; Velez-Pelez, Alejandra; Orton, Frances; Iguchi, Taisen; Mitsui, Naoko; Tooi, Osamu

    2015-07-01

    Anuran amphibians are often present in agricultural landscapes and may therefore be exposed to chemicals in surface waters used for breeding. We used passive accumulation devices (SPMD and POCIS) to sample contaminants from nine breeding sites of the Common toad (Bufo bufo) across England and Wales, measuring endocrine activity of the extracts in a recombinant yeast androgen screen (YAS) and yeast estrogen screen (YES) and an in vitro vitellogenin induction screen in primary culture of Xenopus laevis hepatocytes. We also assessed hatching, growth, survival, and development in caged larvae in situ, and sampled metamorphs for gonadal histopathology. None of the SPMD extracts exhibited estrogen receptor or androgen receptor agonist activity, while POCIS extracts from two sites in west-central England exhibited concentration-dependent androgenic activity in the YAS. Three sites exhibited significant estrogenic activity in both the YES and the Xenopus hepatocyte. Hatching rates varied widely among sites, but there was no consistent correlation between hatching rate and intensity of agricultural activity, predicted concentrations of agrochemicals, or endocrine activity measured in YES/YAS assays. While a small number of intersex individuals were observed, their incidence could not be associated with predicted pesticide exposure or endocrine activitity measured in the in vitro screens. There were no significant differences in sex ratio, as determined by gonadal histomorphology among the study sites, and no significant correlation was observed between proportion of males and predicted exposure to agrochemicals. However, a negative correlation did become apparent in later sampling periods between proportion of males and estrogenic activity of the POCIS sample, as measured in the YES. Our results suggest that larval and adult amphibians may be exposed to endocrine disrupting chemicals in breeding ponds, albeit at low concentrations, and that chemical contaminants other than

  1. Functional Metagenomics: Construction and High-Throughput Screening of Fosmid Libraries for Discovery of Novel Carbohydrate-Active Enzymes.

    Science.gov (United States)

    Ufarté, Lisa; Bozonnet, Sophie; Laville, Elisabeth; Cecchini, Davide A; Pizzut-Serin, Sandra; Jacquiod, Samuel; Demanèche, Sandrine; Simonet, Pascal; Franqueville, Laure; Veronese, Gabrielle Potocki

    2016-01-01

    Activity-based metagenomics is one of the most efficient approaches to boost the discovery of novel biocatalysts from the huge reservoir of uncultivated bacteria. In this chapter, we describe a highly generic procedure of metagenomic library construction and high-throughput screening for carbohydrate-active enzymes. Applicable to any bacterial ecosystem, it enables the swift identification of functional enzymes that are highly efficient, alone or acting in synergy, to break down polysaccharides and oligosaccharides.

  2. Phytochemical Screening, Physicochemical Properties, Acute Toxicity Testing and Screening of Hypoglycaemic Activity of Extracts of Eremurus himalaicus Baker in Normoglycaemic Wistar Strain Albino Rats

    Directory of Open Access Journals (Sweden)

    Ahlam Mushtaq

    2014-01-01

    Full Text Available In the present study EtOAc, MeOH, and aqueous extracts of Eremurus himalaicus were evaluated for hypoglycaemic effect in normal rats using both oral glucose tolerance test and 14-day oral administration study. Phytochemical and physicochemical screening was also done. In oral glucose tolerance test the aqueous and MeOH extracts of Eremurus himalaicus at a dose level of 500 mg/kg body weight prior to glucose load resulted in a significant fall in blood glucose level within 150 min. of glucose administration. The aqueous extract at a dose level of 250 mg/kg body weight and 500 mg/kg body weight also showed good hypoglycaemic response (P < 0.001; this was followed by MeOH extract at a dose level of 500 mg/kg body weight (P < 0.05, while MeOH extract at dose level of 250 mg/kg body weight and ethyl acetate extract at dose level of 250 mg/kg body weight and 500 mg/kg body weight exhibited insignificant effect. Phytochemical screening of extracts revealed the presence of alkaloids, terpenoids, phenolics, tannins, saponins, cardiac glycosides, and flavonoids. The results indicate that aqueous extract possess significant hypoglycaemic activity in normoglycaemic rats which may be attributed to the above-mentioned chemical constituents.

  3. Cardiorespiratory fitness in Flemish adolescents and its relationship with leisure-time physical activity, active travel to school and screen-based sedentariness

    OpenAIRE

    Seghers, Jan; Rutten, Cindy

    2010-01-01

    Introduction Cardiorespiratory fitness is a key component of overall physical fitness and has been identified as a powerful health index in youth (Anderssen et al., 2007). The apparently obvious positive association between cardiorespiratory fitness and physical activity still requires further research. Therefore, the main objective of this study was to evaluate the association of cardiorespiratory fitness with leisure-time physical activity, active travel to school and screen-based sedent...

  4. Research status of defensins and cathelicidins/LL-37 in pulmonary anti-infection immune defense%防御素和cathelicidins/LL-37在肺部抗感染防御中的研究现状

    Institute of Scientific and Technical Information of China (English)

    郭书真; 李昌崇; 林立

    2014-01-01

    抗菌肽是宿主防御系统的重要组成部分.在人气道上皮中主要表达2种阳离子小分子抗菌肽,即防御素和cathelicidins/LL-37,它们通过直接杀菌、调节天然或适应性免疫、损伤修复等生物学活性对抗肺部常见病原体的侵袭.本文就防御素和cathelicidins/LL-37的来源及结构特征、表达调节、在肺部抗感染免疫防御中的作用进行综述.%Antimicrobial protein/peptides (AMPs) are an important part of the defense system.Defensins and cathelicidins/LL-37 are the two main small cationic AMPs which are present in airway epithelial cells.AMPs play a critical role in resisting pathongens of invading lung through direct antimicrobial activity,modulating innate or adaptive immunity,and wound repair.The orign and architectural feature,expression regulation and research progress in pulmonary anti-infection immune defense of defensins and cathelicidins/LL-37 are reviewed here.

  5. Preliminary phytochemical screening and In vitro antioxidant activities of the aqueous extract of Helichrysum longifolium DC

    Directory of Open Access Journals (Sweden)

    Okoh Anthony I

    2010-05-01

    Full Text Available Abstract Background Many oxidative stress related diseases are as a result of accumulation of free radicals in the body. A lot of researches are going on worldwide directed towards finding natural antioxidants of plants origins. The aims of this study were to evaluate in vitro antioxidant activities and to screen for phytochemical constituents of Helichrysum longifolium DC. [Family Asteraceae] aqueous crude extract. Methods We assessed the antioxidant potential and phytochemical constituents of crude aqueous extract of Helichrysum longifolium using tests involving inhibition of superoxide anions, DPPH, H2O2, NO and ABTS. The flavonoid, proanthocyanidin and phenolic contents of the extract were also determined using standard phytochemical reaction methods. Results Phytochemical analyses revealed the presence of tannins, flavonoids, steroids and saponins. The total phenolic content of the aqueous leaf extract was 0.499 mg gallic acid equivalent/g of extract powder. The total flavonoid and proanthocyanidin contents of the plant were 0.705 and 0.005 mg gallic acid equivalent/g of extract powder respectively. The percentage inhibition of lipid peroxide at the initial stage of oxidation showed antioxidant activity of 87% compared to those of BHT (84.6% and gallic acid (96%. Also, the percentage inhibition of malondialdehyde by the extract showed percentage inhibition of 78% comparable to those of BHT (72.24% and Gallic (94.82%. Conclusions Our findings provide evidence that the crude aqueous extract of H. longifolium is a potential source of natural antioxidants, and this justified its uses in folkloric medicines.

  6. Evaluation of Antibacterial Activity and Preliminary Phytochemical Screening of Moringa oleifera on Pathogenic Bacteria

    Directory of Open Access Journals (Sweden)

    Ogah James Ode

    2015-11-01

    Full Text Available The use of higher plants and their extracts to treat infections is an old practice in traditional African medicine. However, scientific research has shown that bioactive compounds in plants are valuable medically in the treatment of infections caused by pathogenic microorganisms. This research work is aimed to evaluate the antibacterial potential of Moringa oleifera extracts on standard microorganisms strains as well as multi-drug resistant strains of medical importance. Acetone, aqueous, ethanol and chloroform extracts of bark, leaves and seeds of Moringa oleifera were investigated for antibacterial activity against Bacillus cereus, Escherichia coli, Klebsiella pneumoniae, Methicillin resistant Staphylococcus aureus (MRSA, Pseudomonas aeruginosa and Proteus mirabilis. The preliminary phytochemical screening and antibacterial assay were carried out using chemicals and agar well diffusion method respectively. The results of phytochemicals analysis revealed differences in the presence of alkaloids, reducing sugars, saponins and volatile oil in all the extracts. Tannins were present in the extract of leaves while terpenes were present in the extract of bark and leaves. Phlobatannins and flavonoids were absent in all the extracts. The antibacterial assay results showed that M. oleifera extracts exhibited broad spectrum activity against four to six bacteria isolates as indicated by the zone of inhibition ranging from 10 to 36mm with variation in the percentage sensitivity of < 100%, = 100% and >100% depending on the plant part and solvent used. The minimum inhibitory concentration (MIC and bactericidal concentration (MBC ranged from 100mg/ml to 450mg/ml and 250mg/ml to 500mg/ml respectively against the isolates used. Standard antibiotic disc (Ofloxacin- 5μg inhibited the growth of all the tested bacteria isolates except P. mirabilis. The results of this research work showed that M. oleifera has great potential as antibacterial compounds against Gram

  7. A High-Throughput Screen Identifies a New Natural Product with Broad-Spectrum Antibacterial Activity

    OpenAIRE

    Patrick Ymele-Leki; Shugeng Cao; Jared Sharp; Kathleen G Lambert; McAdam, Alexander J.; Husson, Robert N.; Giselle Tamayo; Jon Clardy; Watnick, Paula I.

    2012-01-01

    Due to the inexorable invasion of our hospitals and communities by drug-resistant bacteria, there is a pressing need for novel antibacterial agents. Here we report the development of a sensitive and robust but low-tech and inexpensive high-throughput metabolic screen for novel antibiotics. This screen is based on a colorimetric assay of pH that identifies inhibitors of bacterial sugar fermentation. After validation of the method, we screened over 39,000 crude extracts derived from organisms t...

  8. Neuroblastoma Screening

    Science.gov (United States)

    ... Health Professional Neuroblastoma Treatment Neuroblastoma Screening Research Neuroblastoma Screening (PDQ®)–Patient Version What is screening? Go to Health Professional Version Screening is looking ...

  9. Screening for larvicidal activity of ethanolic and aqueous extracts of selected plants against Aedes aegypti and Aedes albopictus larvae

    Institute of Scientific and Technical Information of China (English)

    Michael RusselleAlvarez; Francisco Heralde III; Noel Quiming

    2016-01-01

    Objective: To screen for larvicidal activity of aqueous and ethanolic extracts (95% ethanol) from Selaginella elmeri, Christella dentata, Elatostema sinnatum, Curculigo capitulata, Euphorbia hirta, Murraya koenigii (M. koenigii), Alpinia speciosa, Cymbopogon citratus, Eucalyptus globulus (E. globulus), Jatropha curcas (J. curcas), Psidium guajava, Gliricidia sepium, Ixora coccinea and Capsicum frutescens (C. frutescens) against Aedes aegypti (A. aegypti) and Aedes albopictus (A. albopictus) 3rd instar larvae. Methods: Ethanolic and aqueous extracts were screened for larvicidal activity by exposing the A. aegypti and A. albopictus 3rd instar larvae (15 larvae per trial, triplicates) for 48 h, counting the mortalities every 24 h. Additionally, phytochemical screening for flavonoids, tannins, alkaloids, anthraquinones, anthrones, coumarins, indoles and steroids were performed on active extracts using spray tests. Results: Against A. aegypti, the three most active extracts were C. frutescens ethanolic (100%after 24 and 48 h), J. curcas ethanolic (84.44% after 24 h and 88.89% after 48 h) and M. koenigii ethanolic (53.33% after 24 h and 71.11% after 48 h). On the other hand, against A. albopictus, the three most active extracts were C. frutescens ethanolic (93.33% after 24 h and 100% after 48 h), J. curcas ethanolic (77.78% after 24 h and 82.22% after 48 h) and E. globulus ethanolic (64.44% after 24 h and 73.33% after 48 h). Phytochemical screening was also performed on the active extracts, revealing alkaloids, tannins, indoles and steroids. Conclusios: The results demonstrate the larvicidal activities of ethanolic extracts of Cymbopogon citratus, Euphorbia hirta, Ixora coccinea, Gliricidia sepium, M. koenigii, E. globulus, J. curcas and C. frutescens against A. aegypti and A. albopictus 3rd instar larvae. These could be used as potential larvicidal agents for the control of these mosquitoes.

  10. The influence of friends and psychosocial factors on physical activity and screen time behavior in adolescents: a mixed-methods analysis.

    Science.gov (United States)

    Garcia, Jeanette M; Sirard, John R; Deutsch, Nancy L; Weltman, Arthur

    2016-08-01

    (1) Determine the association between adolescent moderate-to-vigorous physical activity (MVPA) and screen time with their nominated friends' behaviors and (2) explore potential mechanisms of friends' social influences on MVPA and screen time. Participants consisted of 152 adolescents (mean age: 14.5 years, 53 % female, 50 % high school, 80 % Caucasian). MVPA was measured with an Actigraph GT3X+ accelerometer. Demographic and psychosocial variables were assessed via questionnaires. Participants nominated up to 5 friends who completed MVPA and screen time questionnaires. A subset of adolescents (n = 108) participated in focus groups that examined potential mechanism of friends' influence on MVPA and screen time. Multiple regression analysis examined the association of demographic, psychological, and nominated friend variables with participants' MVPA and screen time. NVivo 10.0 was used to analyze qualitative data. Greater levels of friends' MVPA was associated with greater levels of MVPA in both males (p friends' screen time was associated with greater levels of screen time in males (p = .04) while psychosocial variables, such as increased screen time enjoyment, were associated with increased screen time in females (p = .01). School level was not associated with either MVPA or screen time. Focus group data indicated that friends positively influenced participants' MVPA through engaging in activity with participants, verbal encouragement, and modeling of MVPA. All participants preferred to be active with friends rather than alone, however, females preferred activity with a close friend while males preferred to be active with a group. Enjoyment of MVPA was the most cited reason for engaging in MVPA with friends. The majority of participants reported friends not having an influence on screen time. Adolescents with active friends are more likely to be physically active and spend less time engaging in screen-based behaviors. Interventions to increase MVPA in

  11. A Modified Reverse One-Hybrid Screen Identifies Transcriptional Activation Domains in PHYTOCHROME-INTERACTING FACTOR 3.

    Science.gov (United States)

    Dalton, Jutta C; Bätz, Ulrike; Liu, Jason; Curie, Gemma L; Quail, Peter H

    2016-01-01

    Transcriptional activation domains (TADs) are difficult to predict and identify, since they are not conserved and have little consensus. Here, we describe a yeast-based screening method that is able to identify individual amino acid residues involved in transcriptional activation in a high throughput manner. A plant transcriptional activator, PIF3 (phytochrome interacting factor 3), was fused to the yeast GAL4-DNA-binding Domain (BD), driving expression of the URA3 (Orotidine 5'-phosphate decarboxylase) reporter, and used for negative selection on 5-fluroorotic acid (5FOA). Randomly mutagenized variants of PIF3 were then selected for a loss or reduction in transcriptional activation activity by survival on FOA. In the process, we developed a strategy to eliminate false positives from negative selection that can be used for both reverse-1- and 2-hybrid screens. With this method we were able to identify two distinct regions in PIF3 with transcriptional activation activity, both of which are functionally conserved in PIF1, PIF4, and PIF5. Both are collectively necessary for full PIF3 transcriptional activity, but neither is sufficient to induce transcription autonomously. We also found that the TAD appear to overlap physically with other PIF3 functions, such as phyB binding activity and consequent phosphorylation. Our protocol should provide a valuable tool for identifying, analyzing and characterizing novel TADs in eukaryotic transcription factors, and thus potentially contribute to the unraveling of the mechanism underlying transcriptional activation. PMID:27379152

  12. A Modified Reverse One-Hybrid Screen Identifies Transcriptional Activation Domains in PHYTOCHROME-INTERACTING FACTOR 3.

    Science.gov (United States)

    Dalton, Jutta C; Bätz, Ulrike; Liu, Jason; Curie, Gemma L; Quail, Peter H

    2016-01-01

    Transcriptional activation domains (TADs) are difficult to predict and identify, since they are not conserved and have little consensus. Here, we describe a yeast-based screening method that is able to identify individual amino acid residues involved in transcriptional activation in a high throughput manner. A plant transcriptional activator, PIF3 (phytochrome interacting factor 3), was fused to the yeast GAL4-DNA-binding Domain (BD), driving expression of the URA3 (Orotidine 5'-phosphate decarboxylase) reporter, and used for negative selection on 5-fluroorotic acid (5FOA). Randomly mutagenized variants of PIF3 were then selected for a loss or reduction in transcriptional activation activity by survival on FOA. In the process, we developed a strategy to eliminate false positives from negative selection that can be used for both reverse-1- and 2-hybrid screens. With this method we were able to identify two distinct regions in PIF3 with transcriptional activation activity, both of which are functionally conserved in PIF1, PIF4, and PIF5. Both are collectively necessary for full PIF3 transcriptional activity, but neither is sufficient to induce transcription autonomously. We also found that the TAD appear to overlap physically with other PIF3 functions, such as phyB binding activity and consequent phosphorylation. Our protocol should provide a valuable tool for identifying, analyzing and characterizing novel TADs in eukaryotic transcription factors, and thus potentially contribute to the unraveling of the mechanism underlying transcriptional activation.

  13. A Modified Reverse One-Hybrid Screen Identifies Transcriptional Activation Domains in PHYTOCHROME-INTERACTING FACTOR 3

    Science.gov (United States)

    Dalton, Jutta C.; Bätz, Ulrike; Liu, Jason; Curie, Gemma L.; Quail, Peter H.

    2016-01-01

    Transcriptional activation domains (TADs) are difficult to predict and identify, since they are not conserved and have little consensus. Here, we describe a yeast-based screening method that is able to identify individual amino acid residues involved in transcriptional activation in a high throughput manner. A plant transcriptional activator, PIF3 (phytochrome interacting factor 3), was fused to the yeast GAL4-DNA-binding Domain (BD), driving expression of the URA3 (Orotidine 5′-phosphate decarboxylase) reporter, and used for negative selection on 5-fluroorotic acid (5FOA). Randomly mutagenized variants of PIF3 were then selected for a loss or reduction in transcriptional activation activity by survival on FOA. In the process, we developed a strategy to eliminate false positives from negative selection that can be used for both reverse-1- and 2-hybrid screens. With this method we were able to identify two distinct regions in PIF3 with transcriptional activation activity, both of which are functionally conserved in PIF1, PIF4, and PIF5. Both are collectively necessary for full PIF3 transcriptional activity, but neither is sufficient to induce transcription autonomously. We also found that the TAD appear to overlap physically with other PIF3 functions, such as phyB binding activity and consequent phosphorylation. Our protocol should provide a valuable tool for identifying, analyzing and characterizing novel TADs in eukaryotic transcription factors, and thus potentially contribute to the unraveling of the mechanism underlying transcriptional activation. PMID:27379152

  14. Electrochemiluminescent Arrays for Cytochrome P450-Activated Genotoxicity Screening. DNA Damage from Benzo[a]pyrene Metabolites

    Science.gov (United States)

    Hvastkovs, Eli G.; So, Minjeong; Krishnan, Sadagopan; Bajrami, Besnik; Tarun, Maricar; Jansson, Ingela; Schenkman, John B.; Rusling, James F.

    2007-01-01

    Arrays suitable for genotoxicity screening are reported that generate metabolites from cytochrome P450 enzymes (CYPs) in thin-film spots. Array spots containing DNA, various human cyt P450s, and electrochemiluminescence (ECL) generating metallopolymer [Ru(bpy)2PVP10]2+ were exposed to H2O2 to activate the enzymes. ECL from all spots was visualized simultaneously using a CCD camera. Using benzo[a]pyrene as a test substrate, enzyme activity for producing DNA damage in the arrays was found in the order CYP1B1 > CYP1A2 > CYP1A1 > CYP2E1 > myoglobin, the same as the order of their metabolic activity. Thus, these arrays estimate the relative propensity of different enzymes to produce genotoxic metabolites. This is the first demonstration of ECL arrays for high-throughput in vitro genotoxicity screening. PMID:17261025

  15. A new versatile microarray-based method for high-throughput screening of carbohydrate-active enzymes

    DEFF Research Database (Denmark)

    Vidal Melgosa, Silvia; Pedersen, Henriette Lodberg; Schückel, Julia;

    2015-01-01

    Carbohydrate-active enzymes have multiple biological roles and industrial applications. Advances in genome and transcriptome sequencing, together with associated bioinformatic tools have identified vast numbers of putative carbohydrate degrading and modifying enzymes including glycoside hydrolases...... and lytic polysaccharide monooxygenases. However, there is a paucity of methods for rapidly screening the activities of these enzymes. By combining the multiplexing capacity of carbohydrate microarrays with the specificity of molecular probes, we have developed a sensitive, high-throughput and versatile...... semi-quantitative enzyme-screening technique which requires low amounts of enzyme and substrate. The method can be used to assess the activities of single enzymes, enzyme cocktails and crude culture broths against single substrates, substrate mixtures and biomass samples. Moreover, we show...

  16. Screening for Antibiotic Activity by Miniaturized Cultivation in Micro-Segmented Flow

    Science.gov (United States)

    Zang, Emerson; Tovar, Miguel; Martin, Karin; Roth, Martin

    Despite arduous dedication of the scientific community during the last decades, most screening efforts failed to reveal new antibiotic substances. Droplet-based microfluidics provide a powerful platform to effectively exploit natural metabolic diversity and revitalize the search for new antimicrobials. In this chapter, we explore main requirements to develop and apply droplet-based microfluidic screening strategies for the discovery of novel antibiotics from natural products.

  17. Associations of physical activity, screen time with depression, anxiety and sleep quality among Chinese college freshmen.

    Directory of Open Access Journals (Sweden)

    Qi Feng

    Full Text Available To investigate the independent and interactive associations of physical activity (PA and screen time (ST with depression, anxiety and sleep quality among Chinese college students.A cross-sectional study was conducted in Wuhan University, China from November to December 2011. The students reported their PA, ST and socio-economic characteristics using self-administered questionnaires. Sleep quality was measured by the Pittsburgh Sleep Quality Index (PSQI. Depression and anxiety were assessed using the Self-rating Depression Scale (SDS and Self-rating Anxiety Scale (SAS, respectively. Multivariate logistic regression models were used to estimate the odds ratios (ORs and 95% confidence intervals (CIs of the independent and interactive relationships of PA and ST with depression, anxiety and sleep quality.A total of 1106 freshmen (471 females and 635 males aged 18.9±0.9 years were included in the study. After adjustment for potential confounders, high PA and low ST were independently associated with significantly lower risks for poor sleep quality (OR: 0.48, 95% CI: 0.30-0.78 and depression (OR: 0.67, 95%CI: 0.44-0.89, respectively. An interactive inverse association was observed for combined effects of PA and low ST on depression (OR: 0.62, 95%CI: 0.40-0.92 and sleep quality (OR: 0.51, 95%CI: 0.27-0.91. No statistically significant associations were found between PA, ST and anxiety among the participants.These findings suggest an independent and interactive relationship of high PA and low ST with significantly reduced prevalence of depressive problems and favorable sleep quality among Chinese college freshmen.

  18. Implementation of a high-throughput screen for identifying small molecules to activate the Keap1-Nrf2-ARE pathway.

    Directory of Open Access Journals (Sweden)

    Kai Connie Wu

    Full Text Available Nuclear factor erythroid 2-related factor 2 (Nrf2 is a transcription factor that induces a battery of cytoprotective genes involved in antioxidant defense through binding to Antioxidant Response Elements (ARE located in the promoter regions of these genes. To identify Nrf2 activators for the treatment of oxidative/electrophilic stress-induced diseases, the present study developed a high-throughput assay to evaluate Nrf2 activation using AREc32 cells that contain a luciferase gene under the control of ARE promoters. Of the 47,000 compounds screened, 238 (top 0.5% hits of the chemicals increased the luminescent signal more than 14.4-fold and were re-tested at eleven concentrations in a range of 0.01-30 µM. Of these 238 compounds, 231 (96% increased the luminescence signal in a concentration-dependent manner. Chemical structure relationship analysis of these 231 compounds indicated enrichment of four chemical scaffolds (diaryl amides and diaryl ureas, oxazoles and thiazoles, pyranones and thiapyranones, and pyridinones and pyridazinones. In addition, 30 of these 231 compounds were highly effective and/or potent in activating Nrf2, with a greater than 80-fold increase in luminescence, or an EC50 lower than 1.6 µM. These top 30 compounds were also screened in Hepa1c1c7 cells for an increase in Nqo1 mRNA, the prototypical Nrf2-target gene. Of these 30 compounds, 17 increased Nqo1 mRNA in a concentration-dependent manner. In conclusion, the present study documents the development, implementation, and validation of a high-throughput screen to identify activators of the Keap1-Nrf2-ARE pathway. Results from this screening identified Nrf2 activators, and provide novel insights into chemical scaffolds that might prevent oxidative/electrophilic stress-induced toxicity and carcinogenesis.

  19. Development of selective blockers for Ca2+-activated Cl- channel using Xenopus laevis oocytes with an improved drug screening strategy

    Directory of Open Access Journals (Sweden)

    Oh Soo-Jin

    2008-10-01

    Full Text Available Abstract Background Ca2+-activated Cl- channels (CaCCs participate in many important physiological processes. However, the lack of effective and selective blockers has hindered the study of these channels, mostly due to the lack of good assay system. Here, we have developed a reliable drug screening method for better blockers of CaCCs, using the endogeneous CaCCs in Xenopus laevis oocytes and two-electrode voltage-clamp (TEVC technique. Results Oocytes were prepared with a treatment of Ca2+ ionophore, which was followed by a treatment of thapsigargin which depletes Ca2+ stores to eliminate any contribution of Ca2+ release. TEVC was performed with micropipette containing chelerythrine to prevent PKC dependent run-up or run-down. Under these conditions, Ca2+-activated Cl- currents induced by bath application of Ca2+ to oocytes showed stable peak amplitude when repetitively activated, allowing us to test several concentrations of a test compound from one oocyte. Inhibitory activities of commercially available blockers and synthesized anthranilic acid derivatives were tested using this method. As a result, newly synthesized N-(4-trifluoromethylphenylanthranilic acid with trifluoromethyl group (-CF3 at para position on the benzene ring showed the lowest IC50. Conclusion Our results provide an optimal drug screening strategy suitable for high throughput screening, and propose N-(4-trifluoromethylphenylanthranilic acid as an improved CaCC blocker.

  20. The influence of friends and psychosocial factors on physical activity and screen time behavior in adolescents: a mixed-methods analysis.

    Science.gov (United States)

    Garcia, Jeanette M; Sirard, John R; Deutsch, Nancy L; Weltman, Arthur

    2016-08-01

    (1) Determine the association between adolescent moderate-to-vigorous physical activity (MVPA) and screen time with their nominated friends' behaviors and (2) explore potential mechanisms of friends' social influences on MVPA and screen time. Participants consisted of 152 adolescents (mean age: 14.5 years, 53 % female, 50 % high school, 80 % Caucasian). MVPA was measured with an Actigraph GT3X+ accelerometer. Demographic and psychosocial variables were assessed via questionnaires. Participants nominated up to 5 friends who completed MVPA and screen time questionnaires. A subset of adolescents (n = 108) participated in focus groups that examined potential mechanism of friends' influence on MVPA and screen time. Multiple regression analysis examined the association of demographic, psychological, and nominated friend variables with participants' MVPA and screen time. NVivo 10.0 was used to analyze qualitative data. Greater levels of friends' MVPA was associated with greater levels of MVPA in both males (p associated with greater levels of screen time in males (p = .04) while psychosocial variables, such as increased screen time enjoyment, were associated with increased screen time in females (p = .01). School level was not associated with either MVPA or screen time. Focus group data indicated that friends positively influenced participants' MVPA through engaging in activity with participants, verbal encouragement, and modeling of MVPA. All participants preferred to be active with friends rather than alone, however, females preferred activity with a close friend while males preferred to be active with a group. Enjoyment of MVPA was the most cited reason for engaging in MVPA with friends. The majority of participants reported friends not having an influence on screen time. Adolescents with active friends are more likely to be physically active and spend less time engaging in screen-based behaviors. Interventions to increase MVPA in youth could be designed to

  1. Real-time fluorometric turn-on assay for protease activity and inhibitor screening with a benzoperylene probe.

    Science.gov (United States)

    Zhou, Chuibei; Li, Wenying; Chen, Jian; Yang, Meiding; Li, Yang; Zhu, Jintao; Yu, Cong

    2014-03-01

    A real-time fluorescence turn-on strategy for protease activity and inhibitor screening has been developed. A negatively charged benzo[ghi]perylene derivative (probe 1) was employed. Protamine is a cationic protein which can induce aggregation of probe 1 via strong electrostatic and hydrophobic interactions. The fluorescence of probe 1 was efficiently quenched. In the presence of a protease, protamine was enzymatically hydrolyzed and probe 1 de-aggregated. The recovery of the probe 1 monomer fluorescence could be detected. The protease activity could be monitored in real-time. In addition, upon addition of a protease inhibitor, the protease-catalyzed hydrolysis was inhibited, which led to a decreased fluorescence recovery. The fluorometric assay thus could also be employed for screening protease inhibitors. PMID:24427771

  2. 'Becquerel screening' device to automatically measure activity level of contaminated soil in flexible containers

    International Nuclear Information System (INIS)

    Contaminated soil and incineration ash collected during offsite decontamination work following the accident at the Fukushima Daiichi Nuclear Power Station of Tokyo Electric Power Co., Inc. is being stored in flexible containers. These containers are managed taking their activity level into account in accordance with the Decontamination Guidelines issued by the Ministry of the Environment. Toshiba has developed the 'Becquerel Screening' device that can automatically measure the activity level of the contents of each flexible container simply by placing the container on a palette, without the need to take samples for analysis from the container. The Becquerel Screening device is expected to contribute not only to improved operational efficiency but also to reduced exposure of operators to radiation, because it eliminates the need for direct contact with contaminated soil and ash. (author)

  3. Screening the active constituents of Chinese medicinal herbs as potent inhibitors of Cdc25 tyrosine phosphatase, an activator of the mitosis-inducing p34cdc2 kinase

    Institute of Scientific and Technical Information of China (English)

    YANG Hua; ZHENG Shu; MEIJER Laurent; LI Shi-min; LECLERC Sophie; YU Lin-lin; CHENG Jin-quan; ZHANG Su-zhan

    2005-01-01

    Objective: To screen and evaluate the active constituents of Chinese medicinal herbs as potent inhibitors of Cdc25phosphatase. Methods: The affinity chromatography purified glutashione-S-transferase/Cdc25A phosphatase fusion protein and Cdc2/cyclin B from the extracts of starfish M phase oocytes are used as the cell cycle-specific targets for screening the antimitotic constituents. We tested 9 extracts isolated from the Chinese medicinal herbs and vegetables including the agents currently used in cancer treatment by measuring the inhibition of Cdc25A phosphatase and Cdc2 kinase activity. The antitumor activity of the extracts was also evaluated by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay and flow cytometry.Results: Cdc25A inhibitory activity and antitumor activity are detected in the extracts isolated from three Chinese medicinal herbs Agrimonapilosa; Herba solani lyrati; Galla chinesis. Conclusion: We found three extracts isolated from Chinese medicinal herbs have potential inhibitory activity of Cdc25 phosphatase using a highly specific mechanism-based screen assay for antimitotic drug discovery.

  4. Rationale for New York City’s Regulations on Nutrition, Physical Activity, and Screen Time in Early Child Care Centers

    OpenAIRE

    Nonas, Cathy; Silver, Lynn D; Kettel Khan, Laura; Leviton, Laura

    2014-01-01

    Childhood obesity is associated with health risks in childhood, and it increases the risk of adult obesity, which is associated with many chronic diseases. Therefore, implementing policies that may prevent obesity at young ages is important. In 2007, the New York City Department of Health and Mental Hygiene implemented new regulations for early childhood centers to increase physical activity, limit screen time, and provide healthful beverage offerings (ie, restrict sugar-sweetened beverages f...

  5. Screening and purification of a novel trypsin inhibitor from Prosopis juliflora seeds with activity toward pest digestive enzymes.

    Science.gov (United States)

    Sivakumar, S; Franco, O L; Tagliari, P D; Bloch, C; Mohan, M; Thayumanavan, B

    2005-08-01

    Several pests are capable of decreasing crop production causing severe economical and social losses. Aiming to find novel molecules that could impede the digestion process of different pests, a screening of alpha-amylase and trypsin-like proteinase inhibitors was carried out in Prosopis juliflora, showing the presence of both in dry seeds. Furthermore, a novel trypsin inhibitor, with molecular mass of 13,292 Da, was purified showing remarkable in vitro activity against T. castaneum and C. maculatus.

  6. In vitro antiplasmodial activity and phytochemical screening of Alstonia boonei De wild used in treating malaria-associated symptoms

    OpenAIRE

    Enemakwu Thomas Andrew; M. M. Adeyemi; Salihu, L

    2015-01-01

    This study investigated the In vitro antiplasmodial activity and phytochemical constituents of the leaves from Alstonia boonei used in the local treatment of malaria. The crude ethanol extract from the medicinal plant (AB-01) was fractionated into ethyl acetate (AB-01-01), chloroform (AB-01-02) and n-hexane (AB-01-03) fractions. In vitro antiplasmodial assays and phytochemical screening of ethyl acetate, chloroform and n-hexane fractions from the plant were further carried out. Alkaloids, sap...

  7. ON THE SUBSTANTIATION OF INITIAL SCREENING GROSS ALPHA ACTIVITY CONCENTRATION LEVEL FOR DRINKING WATER SAFETY ASSESSMENT ESTABLISHMENT

    Directory of Open Access Journals (Sweden)

    I. K. Romanovich

    2009-01-01

    Full Text Available The present work gives an analysis of the data on natural radionuclides content in drinking-water of Russian Federation groundwater supplies obtained in long-term investigations. On the basis of the mentioned analysis estimation of population internal exposure doses from the drinking-water consumption is carried out and optimal value for initial screening gross alpha activity concentration level is suggested. 

  8. High-Throughput Screening of a Collection of Known Pharmacologically Active Small Compounds for Identification of Candida albicans Biofilm Inhibitors

    OpenAIRE

    Siles, Samuel A.; Srinivasan, Anand; Pierce, Christopher G.; Lopez-Ribot, José L.; Anand K. Ramasubramanian

    2013-01-01

    Candida albicans is the most common etiologic agent of systemic fungal infections with unacceptably high mortality rates. The existing arsenal of antifungal drugs is very limited and is particularly ineffective against C. albicans biofilms. To address the unmet need for novel antifungals, particularly those active against biofilms, we have screened a small molecule library consisting of 1,200 off-patent drugs already approved by the Food and Drug Administration (FDA), the Prestwick Chemical L...

  9. Screening Active Compounds from Garcinia Species Native to China Reveals Novel Compounds Targeting the STAT/JAK Signaling Pathway

    OpenAIRE

    Linfeng Xu; Yuanzhi Lao; Yanhui Zhao; Jian Qin; Wenwei Fu; Yingjia Zhang; Hongxi Xu

    2015-01-01

    Natural compounds from medicinal plants are important resources for drug development. In a panel of human tumor cells, we screened a library of the natural products from Garcinia species which have anticancer potential to identify new potential therapeutic leads and discovered that caged xanthones were highly effective at suppressing multiple cancer cell lines. Their anticancer activities mainly depended on apoptosis pathways. For compounds in sensitive cancer line, their mechanisms of mode o...

  10. Screening for Anthelminthic Activities from Extracts of Zanthoxylum Zanthoxyloides, Neocarya Macrophylla and Celosia Laxa Against Ascaris Infection in Rabbits

    OpenAIRE

    B B Barnabas; Mann, A.; T S Ogunrinola; P E Anyanwu

    2010-01-01

    Summary: Extracts of Celosia laxa, Neocarya macrophylla and Zanthoxylum zanthoxyloides leaves were screened for anthelminthic activities on Ascaris lumbricoides. Celosia laxa appeared to be more potent against A. lumbricoides with rapid recovery of weight while Z. zanthoxyloides has the lowest potency. The effects of these plant extracts on Ascaris lumbricoides suggest that they could serve as an alternative source of anthelminthic agent. Industrial relevance: Infectious diseases pose serio...

  11. Screening of phytochemicals and antimicrobial activity of Caulerpa scalpelliformis collected from Manapad Coast, Tuticorin District, Tamilnadu, South India

    Institute of Scientific and Technical Information of China (English)

    N Karthick; M Anees Fathimal; K Ramesh; H Sridhar; M Natrajan; VV Divya; M Umavanitha; S Umamaheswari

    2014-01-01

    Objective:To analyse the phytochemicals, elements and evaluate the antimicrobial activity of Caulerpa scalpelliformis (C. scalpelliformis) against different bacterial and fungal pathogens. Methods: For the elemental analysis and the screening of phytochemicals, some common and available standard tests were done. The antimicrobial activity was done through the agar well diffusion method. Results:In the qualitative phytochemical screening, among the five different solvent extracts of C. scalpelliformis, the benzene extract showed a maximum number of compounds such as tannins, flavanoids, glycosides, phenols, saponins, terpenoids, etc. The quantitative analysis showed the total protein, total carbohydrate and total lipid content to be (15.86±1.13)%w/w, (10.32±0.94)%w/w, and (1.05±0.08)% w/w respectively. The antibacterial activity showed a maximum zone of inhibition (15±0.18) mm and a minimum zone of inhibition (6±0.05) mm in the benzene extract of C. scalpelliformis exhibited against Serratia marcescens and Bacillus subtilis. The antifungal assay of C. scalpelliformis showed the benzene extract rendered a maximum activity (20±0.25) mm against Aspergillus terreus whereas a minimum activity (12±0.14) mm obtained in the chloroform extract against Aspergillus flavus. Conclusions: Our findings provide the evidence that the benzene extract of C. scalpelliformis possesses the good antimicrobial activity and hence the algae proves to be an effective therapeutic agent.

  12. Isolation, screening, and characterization of surface-active agent-producing, oil-degrading marine bacteria of Mumbai Harbor.

    Science.gov (United States)

    Mohanram, Rajamani; Jagtap, Chandrakant; Kumar, Pradeep

    2016-04-15

    Diverse marine bacterial species predominantly found in oil-polluted seawater produce diverse surface-active agents. Surface-active agents produced by bacteria are classified into two groups based on their molecular weights, namely biosurfactants and bioemulsifiers. In this study, surface-active agent-producing, oil-degrading marine bacteria were isolated using a modified Bushnell-Haas medium with high-speed diesel as a carbon source from three oil-polluted sites of Mumbai Harbor. Surface-active agent-producing bacterial strains were screened using nine widely used methods. The nineteen bacterial strains showed positive results for more than four surface-active agent screening methods; further, these strains were characterized using biochemical and nucleic acid sequencing methods. Based on the results, the organisms belonged to the genera Acinetobacter, Alcanivorax, Bacillus, Comamonas, Chryseomicrobium, Halomonas, Marinobacter, Nesterenkonia, Pseudomonas, and Serratia. The present study confirmed the prevalence of surface-active agent-producing bacteria in the oil-polluted waters of Mumbai Harbor. PMID:26912197

  13. Screening of phytochemicals and antimicrobial activity of Caulerpa scalpelliformis collected from Manapad Coast, Tuticorin District, Tamilnadu, South India

    Directory of Open Access Journals (Sweden)

    N Karthick

    2014-02-01

    Full Text Available Objective: To analyse the phytochemicals, elements and evaluate the antimicrobial activity of Caulerpa scalpelliformis (C. scalpelliformis against different bacterial and fungal pathogens. Methods: For the elemental analysis and the screening of phytochemicals, some common and available standard tests were done. The antimicrobial activity was done through the agar well diffusion method. Results: In the qualitative phytochemical screening, among the five different solvent extracts of C. scalpelliformis, the benzene extract showed a maximum number of compounds such as tannins, flavanoids, glycosides, phenols, saponins, terpenoids, etc. The quantitative analysis showed the total protein, total carbohydrate and total lipid content to be (15.86±1.13% w/w, (10.32±0.94% w/ w, and (1.05±0.08% w/w respectively. The antibacterial activity showed a maximum zone of inhibition (15±0.18 mm and a minimum zone of inhibition (6±0.05 mm in the benzene extract of C. scalpelliformis exhibited against Serratia marcescens and Bacillus subtilis. The antifungal assay of C. scalpelliformis showed the benzene extract rendered a maximum activity (20±0.25 mm against Aspergillus terreus whereas a minimum activity (12±0.14 mm obtained in the chloroform extract against Aspergillus flavus. Conclusions: Our findings provide the evidence that the benzene extract of C. scalpelliformis possesses the good antimicrobial activity and hence the algae proves to be an effective therapeutic agent.

  14. Screening for Anthelminthic Activities from Extracts of Zanthoxylum Zanthoxyloides, Neocarya Macrophylla and Celosia Laxa Against Ascaris Infection in Rabbits

    Directory of Open Access Journals (Sweden)

    B B Barnabas

    2010-12-01

    Full Text Available Summary: Extracts of Celosia laxa, Neocarya macrophylla and Zanthoxylum zanthoxyloides leaves were screened for anthelminthic activities on Ascaris lumbricoides. Celosia laxa appeared to be more potent against A. lumbricoides with rapid recovery of weight while Z. zanthoxyloides has the lowest potency. The effects of these plant extracts on Ascaris lumbricoides suggest that they could serve as an alternative source of anthelminthic agent. Industrial relevance: Infectious diseases pose serious challenges to global health care delivery. Moreoever, in developing countries, the cost of orthodox medication is out of reach of the common man, especially those in rural areas. This is coupled with the adulterated drugs and emergences of drug resistant strains have led to an intensive search for natural products of higher plants, which are biologically active against parasitic infections. Many plants are used locally in traditional medicine to treat parasitic infections. Nigeria offers a rich floral diversity that are used traditionally to treat worm infections. Nigerian medicinal plants (Celosia laxa, Neocarya macrophylla, Zanthoxylum zanthoxyloides used commonly used in Bida, Niger State, Nigeria for the treatment of worm infections were screened for anthelminthic activity. The extracts exhibited varying degree of anthelminthic activities against Ascaris lumbricoides. The extract of C. laxa display potent anthelminthic property. The extract of C. laxa with pronounced activity against A. lumbricoides may contain metabolites that have pharmacologically active principles with promising anthelminthic properties. This indicates the medical potential of C. laxa in the treatment of helminthiasis.

  15. Antifungal activity and phytochemical screening of extracts from Phoenix dactylifera L. cultivars.

    Science.gov (United States)

    Boulenouar, Noureddine; Marouf, Abderrazak; Cheriti, Abdelkrim

    2011-12-01

    In this study, the rachis extracts of eight date palm Phoenix dactylifera L. cultivars were analysed by phytochemical screening and bioautography on Fusarium oxysporum f. sp. albedinis (Foa). The choice of cultivars was based on their reaction to Foa (resistant, tolerant and sensitive). Phytochemical screening was realised for flavonoids, tannins, alkaloids and coumarins. Antifungal effects were mostly represented by dichloromethanic extracts (seven out of nine inhibition zones). The best results were represented by the dichloromethanic extract of the cultivar 'Bent-Cherk' rachis (6.50 ± 1.41 mm) and the ethyl acetate extract of the cultivar 'Rotbi' rachis (6.00 ± 1.41 mm). The date palm cultivars presented some similarities concerning phytochemical screening results related to their resistance or sensibility to Foa. From the correlation between phytochemical screening and bioautography, it was observed that the majority of bioactive compounds against Foa seem to be polyphenols. Thus, the natural defence mechanism in vivo against Foa is probably related to the action of polyphenols. The difference between resistant, tolerant and sensitive cultivars is related to their mechanism of action. PMID:21834627

  16. Home environment relationships with children’s physical activity, sedentary time, and screen time by socioeconomic status

    Directory of Open Access Journals (Sweden)

    Tandon Pooja S

    2012-07-01

    Full Text Available Abstract Background Children in households of lower socioeconomic status (SES are more likely to be overweight/obese. We aimed to determine if home physical activity (PA environments differed by SES and to explore home environment mediators of the relation of family SES to children’s PA and sedentary behavior. Methods Participants were 715 children aged 6 to 11 from the Neighborhood Impact on Kids (NIK Study. Household SES was examined using highest educational attainment and income. Home environment was measured by parent report on a survey. Outcomes were child’s accelerometer-measured PA and parent-reported screen time. Mediation analyses were conducted for home environment factors that varied by SES. Results Children from lower income households had greater media access in their bedrooms (TV 52% vs. 14%, DVD player 39% vs. 14%, video games 21% vs. 9% but lower access to portable play equipment (bikes 85% vs. 98%, jump ropes 69% vs. 83% compared to higher income children. Lower SES families had more restrictive rules about PA (2.5 vs. 2.0. Across SES, children watched TV/DVDs with parents/siblings more often than they engaged in PA with them. Parents of lower SES watched TV/DVDs with their children more often (3.1 vs. 2.5 days/week. Neither total daily and home-based MVPA nor sedentary time differed by SES. Children’s daily screen time varied from 1.7 hours/day in high SES to 2.4 in low SES families. Media in the bedroom was related to screen time, and screen time with parents was a mediator of the SES--screen time relationship. Conclusions Lower SES home environments provided more opportunities for sedentary behavior and fewer for PA. Removing electronic media from children’s bedrooms has the potential to reduce disparities in chronic disease risk.

  17. piggyBac transposon somatic mutagenesis with an activated reporter and tracker (PB-SMART for genetic screens in mice.

    Directory of Open Access Journals (Sweden)

    Sean F Landrette

    Full Text Available Somatic forward genetic screens have the power to interrogate thousands of genes in a single animal. Retroviral and transposon mutagenesis systems in mice have been designed and deployed in somatic tissues for surveying hematopoietic and solid tumor formation. In the context of cancer, the ability to visually mark mutant cells would present tremendous advantages for identifying tumor formation, monitoring tumor growth over time, and tracking tumor infiltrations and metastases into wild-type tissues. Furthermore, locating mutant clones is a prerequisite for screening and analyzing most other somatic phenotypes. For this purpose, we developed a system using the piggyBac (PB transposon for somatic mutagenesis with an activated reporter and tracker, called PB-SMART. The PB-SMART mouse genetic screening system can simultaneously induce somatic mutations and mark mutated cells using bioluminescence or fluorescence. The marking of mutant cells enable analyses that are not possible with current somatic mutagenesis systems, such as tracking cell proliferation and tumor growth, detecting tumor cell infiltrations, and reporting tissue mutagenesis levels by a simple ex vivo visual readout. We demonstrate that PB-SMART is highly mutagenic, capable of tumor induction with low copy transposons, which facilitates the mapping and identification of causative insertions. We further integrated a conditional transposase with the PB-SMART system, permitting tissue-specific mutagenesis with a single cross to any available Cre line. Targeting the germline, the system could also be used to conduct F1 screens. With these features, PB-SMART provides an integrated platform for individual investigators to harness the power of somatic mutagenesis and phenotypic screens to decipher the genetic basis of mammalian biology and disease.

  18. Electrochemiluminescent Arrays for Cytochrome P450-Activated Genotoxicity Screening. DNA Damage from Benzo[a]pyrene Metabolites

    OpenAIRE

    Hvastkovs, Eli G.; So, Minjeong; Krishnan, Sadagopan; Bajrami, Besnik; Tarun, Maricar; Jansson, Ingela; Schenkman, John B.; Rusling, James F.

    2007-01-01

    Arrays suitable for genotoxicity screening are reported that generate metabolites from cytochrome P450 enzymes (CYPs) in thin-film spots. Array spots containing DNA, various human cyt P450s, and electrochemiluminescence (ECL) generating metallopolymer [Ru(bpy)2PVP10]2+ were exposed to H2O2 to activate the enzymes. ECL from all spots was visualized simultaneously using a CCD camera. Using benzo[a]pyrene as a test substrate, enzyme activity for producing DNA damage in the arrays was found in th...

  19. BIOCHEMICAL GENETIC STUDIES ON CUTYLEFISH SEPIELLA MAINDRONI (CEPHALOPODA: SEPIIDAE)——ACTIVE LOCI SCREENING OF ISOZYME

    Institute of Scientific and Technical Information of China (English)

    郑小东; YutakaNatsukari; 王如才; 王昭萍; 李云

    2001-01-01

    Screening of 46 putative enzyme-coding loci and 4 different kinds of tissues of Sepiella maindroni de Rochebrone, 1884 for enzymatic activities using starch gel electrophoretic technique proved that the 21 enzymes such as AAT, AK, ALP, AP, CK, DIA, ES, FBP, G3PDH, GPI, GRS,IDH, LDH, MDH, MEP, MPI, NP, PGDH, PGM, SOD and XO* , were active to Sepiella maindroni after being stained. The tissue exhibiting stable and clear bands was also determined. Among tissues tested, mantle muscle tissue was the best for electrophoretic survey of isozymes. Buccal bulb muscle, eye and liver were fairly good for some special enzymes, such as DIA, ES, MPI, NT, etc.

  20. New classes of alanine racemase inhibitors identified by high-throughput screening show antimicrobial activity against Mycobacterium tuberculosis.

    Directory of Open Access Journals (Sweden)

    Karen G Anthony

    Full Text Available BACKGROUND: In an effort to discover new drugs to treat tuberculosis (TB we chose alanine racemase as the target of our drug discovery efforts. In Mycobacterium tuberculosis, the causative agent of TB, alanine racemase plays an essential role in cell wall synthesis as it racemizes L-alanine into D-alanine, a key building block in the biosynthesis of peptidoglycan. Good antimicrobial effects have been achieved by inhibition of this enzyme with suicide substrates, but the clinical utility of this class of inhibitors is limited due to their lack of target specificity and toxicity. Therefore, inhibitors that are not substrate analogs and that act through different mechanisms of enzyme inhibition are necessary for therapeutic development for this drug target. METHODOLOGY/PRINCIPAL FINDINGS: To obtain non-substrate alanine racemase inhibitors, we developed a high-throughput screening platform and screened 53,000 small molecule compounds for enzyme-specific inhibitors. We examined the 'hits' for structural novelty, antimicrobial activity against M. tuberculosis, general cellular cytotoxicity, and mechanism of enzyme inhibition. We identified seventeen novel non-substrate alanine racemase inhibitors that are structurally different than any currently known enzyme inhibitors. Seven of these are active against M. tuberculosis and minimally cytotoxic against mammalian cells. CONCLUSIONS/SIGNIFICANCE: This study highlights the feasibility of obtaining novel alanine racemase inhibitor lead compounds by high-throughput screening for development of new anti-TB agents.

  1. Role of antioxidative enzymes activity in salt stress and salinity screening in rice grown under in vitro condition

    Directory of Open Access Journals (Sweden)

    G.Thamodharan* And M. Arumugam Pillai

    2014-09-01

    Full Text Available Role of antioxidative enzyme activity in salt stress and salinity screening was studied in the callus of two rice cultivars (White ponni and BPT-5204. The antioxidant activities of the rice callus were determined by analyzing three enzymes activity namely, Superoxide Dismutase (SOD, Catalase (CAT and Ascorbate Peroxidase (APX grown under saline condition. Enzymes were analysed in 15 days old rice callus culture grown under salt stress and non-saline conditions. All the three enzyme activities were varied according to salt concentrations in the medium. SOD and CAT activities were higher in BPT-5204 but APX activities were higher in White ponni. Among the NaCl treatment, medium containing 40 mM NaCl observed higher enzyme activity than 20 and 30 mM NaCl. Under non saline condition there is no significant difference was noticed in the enzymatic activities and callus growth parameter in both the cultivars. Observation was carried out on the change in callus growth parameter like weight and color of the callus. There was a significant reduction in weight and also change in colour of the callus was noticed with respect to higher salt concentrations (30 and 40 mM NaCl in the medium for both the cultivars. The observed data indicated that rice plant responds well to salt-induced oxidative stress by increasing their enzymatic antioxidant defense systems. The antioxidant enzyme activity play vital role in defense against salt stress and this may help to screen the salt tolerant line grown under in vitro condition in early callus stage itself.

  2. Soluble urokinase plasminogen activator receptor as a prognostic marker in men participating in prostate cancer screening

    DEFF Research Database (Denmark)

    Kjellman, A; Akre, O; Gustafsson, O;

    2011-01-01

    with prostate cancer and cardiovascular disease mortality. METHODS: Using time-resolved fluorescence immunoassays, we measured intact suPAR [suPAR(I-III)] and intact plus cleaved suPAR [suPAR(I-III) + suPAR(II-III)] and thus calculated the amount of suPAR(II-III) in serum samples from 375 men participating...... in a prostate cancer screening trial. A total of 312 men were free of prostate cancer and 63 men had prostate cancer diagnosed at the time of screening. The cohort was followed for 15 years. We assessed survival using Kaplan-Meier estimation and Cox proportional hazards regression. RESULTS: The mean age...... at blood sampling was 64 years. In total, 152 men died during follow-up. SuPAR(I-III) and suPAR(II-III) were significantly positively associated with mortality (P = 0.001 and P prostate cancer status, an increase in su...

  3. A Simple Assay to Screen Antimicrobial Compounds Potentiating the Activity of Current Antibiotics

    OpenAIRE

    Junaid Iqbal; Ruqaiyyah Siddiqui; Shahana Urooj Kazmi; Naveed Ahmed Khan

    2013-01-01

    Antibiotic resistance continues to pose a significant problem in the management of bacterial infections, despite advances in antimicrobial chemotherapy and supportive care. Here, we suggest a simple, inexpensive, and easy-to-perform assay to screen antimicrobial compounds from natural products or synthetic chemical libraries for their potential to work in tandem with the available antibiotics against multiple drug-resistant bacteria. The aqueous extract of Juglans regia tree bark was tested a...

  4. Screening of xylanase activity of Streptomyces albidoflavus PSM-3n isolated from Uttarakhand

    OpenAIRE

    Pushpendra Sharma; Vijay Kumar; Bindu Naik; Gajraj Singh Bisht

    2013-01-01

    Background: Awareness towards the environmental pollution had made the evolution of green technology by which enzymes got special attention in industries. The enzymes replaced chemical catalysts in manufacturing various chemicals, agricultural and pharmaceutical products. Material and methods: Actinomycetes were isolated and screened for their ability to produce xylanase. For the most promising isolate, selection of media, effect of pH, temperature, metal ions, and detergents on enzyme pro...

  5. Screening for lead compounds and herbal extracts with potential anti-influenza viral activity.

    Science.gov (United States)

    Klaywong, Konrapob; Khutrakul, Gachagorn; Choowongkomon, Kiattawee; Lekcharoensuk, Chalermpol; Petcharat, Nantawan; Leckcharoensuk, Porntippa; Ramasoota, Pongrama

    2014-01-01

    Nonstructural protein 1 (NS1) of the highly pathogenic avian influenza virus (H5N1) contains a conserved RNA binding domain (RBD) that inhibits antiviral functions of host-innate immune response. Dimerization of NS1 forms a central groove and binds to double stranded (ds) RNA. This region might serve as a potential drug target. In this study, three dimensional structure model of NS1 RBD protein was constructed and virtual screening was performed to identify lead compounds that bound within and around the central groove. The virtual screening showed that 5 compounds bound within the central groove with binding energy ranging between -16.05 and -17.36 Kcal/mol. Two commercially available compounds, estradiol and veratridine, were selected for using in an in vitro screening assay. The results showed that neither of the compounds could inhibit the association between dsRNA and NS1 RBD protein. In addition, 34 herbal extracts were examined for their inhibitory effects. Five of them were able to inhibit association between NS1 RBD and dsRNA in electrophoresis mobility shift assay. Four herbs, Terminalia belirica, Salacia chinensis, Zingiber montanum and Peltophorum pterocarpum, could reduce > 50% of infectivity of H5N1 in a cell-based assay, and it is worth further studying their potential use as source of antiviral drugs. PMID:24964655

  6. A High-affinity Activator of G551D-CFTR Chloride Channel Identified By High Throughput Screening

    Institute of Scientific and Technical Information of China (English)

    ZHAO Lu; HE Cheng-yan; LIU Yan-li; ZHOU Hong-lan; ZHOU Jin-song; SHANG De-jing; YANG Hong

    2004-01-01

    A stably transfected CHO cell line coexpressing G551D-CFTR and iodide-sensitive yellow fluorescent protein mutant EYFP-H148Q-I152L was successfully established and used as assay model to identify small-molecule activators of G551D-CFTR chloride channel from 100000 diverse combinatorial compounds by high throughput screening on a customized Beckman robotic system. A bicyclooctane compound was identified to activate G551D-CFTR chloride channel with high-affinity(Kd=1.8 μmol/L). The activity of the bicyclooctane compound is G551D-CFTR-specific, reversible and non-toxic. The G551D-CFTR activator may be useful as a tool to study the mutant G551D-CFTR chloride channel structure and transport properties and as a candidate drug to cure cystic fibrosis caused by G551D-CFTR mutation.

  7. Pharmacophore-based virtual screening, biological evaluation and binding mode analysis of a novel protease-activated receptor 2 antagonist.

    Science.gov (United States)

    Cho, Nam-Chul; Seo, Seoung-Hwan; Kim, Dohee; Shin, Ji-Sun; Ju, Jeongmin; Seong, Jihye; Seo, Seon Hee; Lee, Iiyoun; Lee, Kyung-Tae; Kim, Yun Kyung; No, Kyoung Tai; Pae, Ae Nim

    2016-08-01

    Protease-activated receptor 2 (PAR2) is a G protein-coupled receptor, mediating inflammation and pain signaling in neurons, thus it is considered to be a potential therapeutic target for inflammatory diseases. In this study, we performed a ligand-based virtual screening of 1.6 million compounds by employing a common-feature pharmacophore model and two-dimensional similarity search to identify a new PAR2 antagonist. The common-feature pharmacophore model was established based on the biological screening results of our in-house library. The initial virtual screening yielded a total number of 47 hits, and additional biological activity tests including PAR2 antagonism and anti-inflammatory effects resulted in a promising candidate, compound 43, which demonstrated an IC50 value of 8.22 µM against PAR2. In next step, a PAR2 homology model was constructed using the crystal structure of the PAR1 as a template to explore the binding mode of the identified ligands. A molecular docking method was optimized by comparing the binding modes of a known PAR2 agonist GB110 and antagonist GB83, and applied to predict the binding mode of our hit compound 43. In-depth docking analyses revealed that the hydrophobic interaction with Phe243(5.39) is crucial for PAR2 ligands to exert antagonistic activity. MD simulation results supported the predicted docking poses that PAR2 antagonist blocked a conformational rearrangement of Na(+) allosteric site in contrast to PAR2 agonist that showed Na(+) relocation upon GPCR activation. In conclusion, we identified new a PAR2 antagonist together with its binding mode, which provides useful insights for the design and development of PAR2 ligands. PMID:27600555

  8. ANTIMICROBIAL ACTIVITIES AND PRELIMINARY PHYTOCHEMICAL SCREENING ON THE CRUDE EXTRACTS OF THE LEAVES OF CINERARIA ABYSSINICA SCH. BIP. EXA. RICH

    Directory of Open Access Journals (Sweden)

    Biruk Sintayehu*, Kaleab Asres and Avijit Mazumder

    2012-05-01

    Full Text Available In Ethiopian traditional medicine, the aqueous decoction of the leaves of Cineraria abyssinica Sch. Bip. exA. Rich (Asteraceae is used for treatments of various ailments including diarrhea, however, to date, there appear to have been no reports on the phytochemistry and the antimicrobial activity of the plant. The main aim of this study was, therefore, to carry out preliminary phytochemical screening and antimicrobial activities on leaf extracts of C. abyssinica. The in vitro antimicrobial activities of the aqueous and 80% methanolic crude extracts of the leaves of C. abyssinica were investigated against Gram positive and Gram negative bacteria by agar disc diffusion method. Both the aqueous and 80% methanolic extracts showed various degrees of potent antibacterial activities comparable to the standard drug ciprofloxacin against all of the bacteria tested except Bacillus species. Preliminary phytochemical screening of the plant revealed the presence of polyphenols, flavonoids, coumarins, saponins, terpenoids and phytosterols. The acute toxicity studies showed the nontoxic nature of the plant up to 3 g/kg. Therefore, the present study revealed for the first time the presence of antimicrobial phytochemicals in the leaves of C. abyssinica that scientifically validated the traditional use and its great potential to be used for treatment of infectious diarrhea.

  9. Identification of active Plasmodium falciparum calpain to establish screening system for Pf-calpain-based drug development

    Directory of Open Access Journals (Sweden)

    Soh Byoung

    2013-02-01

    Full Text Available Abstract Background With the increasing resistance of malaria parasites to available drugs, there is an urgent demand to develop new anti-malarial drugs. Calpain inhibitor, ALLN, is proposed to inhibit parasite proliferation by suppressing haemoglobin degradation. This provides Plasmodium calpain as a potential target for drug development. Pf-calpain, a cysteine protease of Plasmodium falciparum, belongs to calpain-7 family, which is an atypical calpain not harboring Ca2+-binding regulatory motifs. In this present study, in order to establish the screening system for Pf-calpain specific inhibitors, the active form of Pf-calpain was first identified. Methods Recombinant Pf-calpain including catalytic subdomain IIa (rPfcal-IIa was heterologously expressed and purified. Enzymatic activity was determined by both fluorogenic substrate assay and gelatin zymography. Molecular homology modeling was carried out to address the activation mode of Pf-calpain in the aspect of structural moiety. Results Based on the measurement of enzymatic activity and protease inhibitor assay, it was found that the active form of Pf-calpain only contains the catalytic subdomain IIa, suggesting that Pf-calpain may function as a monomeric form. The sequence prediction indicates that the catalytic subdomain IIa contains all amino acid residues necessary for catalytic triad (Cys-His-Asn formation. Molecular modeling suggests that the Pf-calpain subdomain IIa makes an active site, holding the catalytic triad residues in their appropriate orientation for catalysis. The mutation analysis further supports that those amino acid residues are functional and have enzymatic activity. Conclusion The identified active form of Pf-calpain could be utilized to establish high-throughput screening system for Pf-calpain inhibitors. Due to its unique monomeric structural property, Pf-calpain could be served as a novel anti-malarial drug target, which has a high specificity for malaria parasite

  10. Mobile input device type, texting style and screen size influence upper extremity and trapezius muscle activity, and cervical posture while texting.

    Science.gov (United States)

    Kietrys, David M; Gerg, Michael J; Dropkin, Jonathan; Gold, Judith E

    2015-09-01

    This study aimed to determine the effects of input device type, texting style, and screen size on upper extremity and trapezius muscle activity and cervical posture during a short texting task in college students. Users of a physical keypad produced greater thumb, finger flexor, and wrist extensor muscle activity than when texting with a touch screen device of similar dimensions. Texting on either device produced greater wrist extensor muscle activity when texting with 1 hand/thumb compared with both hands/thumbs. As touch screen size increased, more participants held the device on their lap, and chose to use both thumbs less. There was also a trend for greater finger flexor, wrist extensor, and trapezius muscle activity as touch screen size increased, and for greater cervical flexion, although mean differences for cervical flexion were small. Future research can help inform whether the ergonomic stressors observed during texting are associated with musculoskeletal disorder risk. PMID:25959323

  11. Research Advances of Aminoacyl-tRNA Synthetase Inhibitors as Novel Anti-infective Agents%氨酰tRNA合成酶抑制剂作为新型抗感染药物的研究进展

    Institute of Scientific and Technical Information of China (English)

    王庆; 孟青青; 周虎臣

    2012-01-01

    Increasing rates of bacterial resistance to known classes of antibiotics present a severe global challenge. As a consequence, the search for new chemical entities that address novel bacterial targets remains ongoing. Aminoacyl-tRNA synthetases (aaRS) catalyze the ligation of amino acids to their cognate tRNAs and they are essential for protein synthesis. Inhibition of aaRS leads to protein synthesis inhibition, which cause cell growth arrest. Consequently, aminoacyl-tRNA synthetase is a class of potential anti-infective target. AaRS inhibitors identified from natural products and their derivatives, substrate and reaction intermediate mimics, synthetic compounds and hits of virtual screening as novel antibacterial and antifungal agents are summarized in this article. The target characteristic, classification and catalytic mechanism of aminoacyl-tRNA synthetases are also introduced.%细菌耐药性的不断上升对现有阶段的抗生素类药物提出了一个严峻的挑战,同时也掀起了针对于新靶标的抗菌药物的研究.氨酰tRNA合成酶(aaRS)催化特定氨基酸连接到相应的tRNA分子上,在蛋白质的合成过程中起着必不可少的作用.氨酰tRNA合成酶的抑制会导致蛋白质合成的停止,扰乱细菌和真菌的生长,因此氨酰tRNA合成酶是一类潜在的抗感染靶标.本文分别综述了天然产物及其衍生的aaRS抑制剂,底物和反应中间体模拟物,通过合成和通过虚拟筛选得到的aaRS抑制剂作为新型抗细菌和抗真菌药物的研究进展,并对aaRS的靶标特点、分类和催化机制作一简要介绍.

  12. Vision Screening

    Science.gov (United States)

    ... offer vision screening programs for children. At what age should a child have his or her vision screened? Vision screening ... a child fails a vision screening at any age, the child should be referred for a comprehensive eye examination. ...

  13. Bioactivity of marine organisms. Part 3. Screening of marine algae of Indian coast for biological activity

    Digital Repository Service at National Institute of Oceanography (India)

    Kamat, S.Y.; Wahidullah, S.; Naik, C.G.; DeSouza, L.; Jayasree, V.; Ambiye, V.; Bhakuni, D.S.; Goel, A.K.; Garg, H.S.; Srimal, R.C.

    were diuretic, 3 hypoglycaemic, 3 hypotensive, 4 exhibited anti- implantation activity, cytokinin activity was observed in one and one showed adrenergic blocking action. The extracts neither , had anti-bacterial, anti-fungal and anti-viral activities...

  14. Biochemical Screening of Five Protein Kinases from Plasmodium falciparum against 14,000 Cell-Active Compounds.

    Directory of Open Access Journals (Sweden)

    Gregory J Crowther

    Full Text Available In 2010 the identities of thousands of anti-Plasmodium compounds were released publicly to facilitate malaria drug development. Understanding these compounds' mechanisms of action--i.e., the specific molecular targets by which they kill the parasite--would further facilitate the drug development process. Given that kinases are promising anti-malaria targets, we screened ~14,000 cell-active compounds for activity against five different protein kinases. Collections of cell-active compounds from GlaxoSmithKline (the ~13,000-compound Tres Cantos Antimalarial Set, or TCAMS, St. Jude Children's Research Hospital (260 compounds, and the Medicines for Malaria Venture (the 400-compound Malaria Box were screened in biochemical assays of Plasmodium falciparum calcium-dependent protein kinases 1 and 4 (CDPK1 and CDPK4, mitogen-associated protein kinase 2 (MAPK2/MAP2, protein kinase 6 (PK6, and protein kinase 7 (PK7. Novel potent inhibitors (IC50 < 1 μM were discovered for three of the kinases: CDPK1, CDPK4, and PK6. The PK6 inhibitors are the most potent yet discovered for this enzyme and deserve further scrutiny. Additionally, kinome-wide competition assays revealed a compound that inhibits CDPK4 with few effects on ~150 human kinases, and several related compounds that inhibit CDPK1 and CDPK4 yet have limited cytotoxicity to human (HepG2 cells. Our data suggest that inhibiting multiple Plasmodium kinase targets without harming human cells is challenging but feasible.

  15. Screening of 397 chemicals and development of a quantitative structure-activity relationship model for androgen receptor antagonism

    DEFF Research Database (Denmark)

    Vinggaard, Annemarie; Niemelä, Jay Russell; Wedebye, Eva Bay;

    2008-01-01

    We have screened 397 chemicals for human androgen receptor (AR) antagonism by a sensitive reporter gene assay to generate data for the development of a quantitative structure-activity relationship (QSAR) model. A total of 523 chemicals comprising data on 292 chemicals from our laboratory and data...... on 231 chemicals from the literature constituted the training set for the model. The chemicals were selected with the purpose of representing a wide range of chemical structures (e.g., organochlorines and polycyclic aromatic hydrocarbons) and various functions (e.g., natural hormones, pesticides......, plastizicers, plastic additives, brominated flame retardants, and roast mutagens). In addition, the intention was to obtain an equal number of positive and negative chemicals. Among our own data for the training set, 45.7% exhibited inhibitory activity against the transcriptional activity induced...

  16. A graphene screen-printed carbon electrode for real-time measurements of unoccupied active sites in a cellulase

    DEFF Research Database (Denmark)

    Cruys-Bagger, Nicolaj; Tatsumi, Hirosuke; Borch, Kim;

    2014-01-01

    . In this work we describe a new electrochemical approach to the quantification of the populations of enzyme that are respectively free in the aqueous bulk, adsorbed to the insoluble substrate with an unoccupied active site or threaded with the cellulose strand in the active tunnel. Distinction of these three...... states appears essential to the idetification of the rate limiting step. The method is based on disposable graphene modified screen-printed carbon electrodes, and we show how the temporal development in the concentrations of the three enzyme forms can be derived from a combination of the electrochemical...... data and adsorption measuments. The approach was tested for the cellobiohydrolase Cel7A from Hypocrea jecorina acting on microcrystalline cellulose, and it was found that the threaded enzyme form dominates for this system while adsorbed enzyme with an unoccupied active site constitutes less than 5...

  17. Preliminary Phytochemical Screening And Evaluation of Free Radical Scavenging Activity Of Stevia rebaudiana Bertoni From Different Geographical Sources

    Directory of Open Access Journals (Sweden)

    Bitasta Mandal

    2013-05-01

    Full Text Available Stevia rebaudiana Bertoni, a natural non-caloric substitute to conventional sugar, is also popular as the “sweet herb of Paraguay”. It is a storehouse of various bioactive constituents mainly, the ent-kaurene diterpene glycosides namely stevioside, rebaudioside A, B, C, D and E. The plant is known to exhibit a wide range of biological activities like hypoglycemic, anti-oxidant, anticancer, antibacterial activities. The present research is based on a preliminary phytochemical screening and comparative evaluation of in vitro antioxidant activity of the dried leaves of five varieties of Stevia rebaudiana procured from five different geographical locations of India viz., Delhi, Surat, Kangra, Bangalore and Indore. Total phenolic and total flavonoid content was also determined using Folin-Ciocalteu reagent method and aluminum chloride colorimetric. The result showed that the variety from Kangra showed the highest phenolic and flavonoid content of 5.87 and 62.22 mg GAE/L respectively.

  18. Screening Active Compounds from Garcinia Species Native to China Reveals Novel Compounds Targeting the STAT/JAK Signaling Pathway

    Directory of Open Access Journals (Sweden)

    Linfeng Xu

    2015-01-01

    Full Text Available Natural compounds from medicinal plants are important resources for drug development. In a panel of human tumor cells, we screened a library of the natural products from Garcinia species which have anticancer potential to identify new potential therapeutic leads and discovered that caged xanthones were highly effective at suppressing multiple cancer cell lines. Their anticancer activities mainly depended on apoptosis pathways. For compounds in sensitive cancer line, their mechanisms of mode of action were evaluated. 33-Hydroxyepigambogic acid and 35-hydroxyepigambogic acid exhibited about 1 μM IC50 values against JAK2/JAK3 kinases and less than 1 μM IC50 values against NCI-H1650 cell which autocrined IL-6. Thus these two compounds provided a new antitumor molecular scaffold. Our report describes 33-hydroxyepigambogic acid and 35-hydroxyepigambogic acid that inhibited NCI-H1650 cell growth by suppressing constitutive STAT3 activation via direct inhibition of JAK kinase activity.

  19. Identification of novel human dipeptidyl peptidase-IV inhibitors of natural origin (part I: virtual screening and activity assays.

    Directory of Open Access Journals (Sweden)

    Laura Guasch

    Full Text Available BACKGROUND: There has been great interest in determining whether natural products show biological activity toward protein targets of pharmacological relevance. One target of particular interest is DPP-IV whose most important substrates are incretins that, among other beneficial effects, stimulates insulin biosynthesis and secretion. Incretins have very short half-lives because of their rapid degradation by DPP-IV and, therefore, inhibiting this enzyme improves glucose homeostasis. As a result, DPP-IV inhibitors are of considerable interest to the pharmaceutical industry. The main goals of this study were (a to develop a virtual screening process to identify potential DPP-IV inhibitors of natural origin; (b to evaluate the reliability of our virtual-screening protocol by experimentally testing the in vitro activity of selected natural-product hits; and (c to use the most active hit for predicting derivatives with higher binding affinities for the DPP-IV binding site. METHODOLOGY/PRINCIPAL FINDINGS: We predicted that 446 out of the 89,165 molecules present in the natural products subset of the ZINC database would inhibit DPP-IV with good ADMET properties. Notably, when these 446 molecules were merged with 2,342 known DPP-IV inhibitors and the resulting set was classified into 50 clusters according to chemical similarity, there were 12 clusters that contained only natural products for which no DPP-IV inhibitory activity has been previously reported. Nine molecules from 7 of these 12 clusters were then selected for in vitro activity testing and 7 out of the 9 molecules were shown to inhibit DPP-IV (where the remaining two molecules could not be solubilized, preventing the evaluation of their DPP-IV inhibitory activity. Then, the hit with the highest activity was used as a lead compound in the prediction of more potent derivatives. CONCLUSIONS/SIGNIFICANCE: We have demonstrated that our virtual-screening protocol was successful in identifying novel

  20. Porcine E. coli: virulence-associated genes, resistance genes and adhesion and probiotic activity tested by a new screening method.

    Science.gov (United States)

    Schierack, Peter; Rödiger, Stefan; Kuhl, Christoph; Hiemann, Rico; Roggenbuck, Dirk; Li, Ganwu; Weinreich, Jörg; Berger, Enrico; Nolan, Lisa K; Nicholson, Bryon; Römer, Antje; Frömmel, Ulrike; Wieler, Lothar H; Schröder, Christian

    2013-01-01

    We established an automated screening method to characterize adhesion of Escherichia coli to intestinal porcine epithelial cells (IPEC-J2) and their probiotic activity against infection by enteropathogenic E. coli (EPEC). 104 intestinal E. coli isolates from domestic pigs were tested by PCR for the occurrence of virulence-associated genes, genes coding for resistances to antimicrobial agents and metals, and for phylogenetic origin by PCR. Adhesion rates and probiotic activity were examined for correlation with the presence of these genes. Finally, data were compared with those from 93 E. coli isolates from wild boars. Isolates from domestic pigs carried a broad variety of all tested genes and showed great diversity in gene patterns. Adhesions varied with a maximum of 18.3 or 24.2 mean bacteria adherence per epithelial cell after 2 or 6 hours respectively. Most isolates from domestic pigs and wild boars showed low adherence, with no correlation between adhesion/probiotic activity and E. coli genes or gene clusters. The gene sfa/foc, encoding for a subunit of F1C fimbriae did show a positive correlative association with adherence and probiotic activity; however E. coli isolates from wild boars with the sfa/foc gene showed less adhesion and probiotic activity than E. coli with the sfa/foc gene isolated from domestic pigs after 6 hour incubation. In conclusion, screening porcine E. coli for virulence associated genes genes, adhesion to intestinal epithelial cells, and probiotic activity revealed a single important adhesion factor, several probiotic candidates, and showed important differences between E. coli of domestic pigs and wild boars.

  1. Porcine E. coli: virulence-associated genes, resistance genes and adhesion and probiotic activity tested by a new screening method.

    Directory of Open Access Journals (Sweden)

    Peter Schierack

    Full Text Available We established an automated screening method to characterize adhesion of Escherichia coli to intestinal porcine epithelial cells (IPEC-J2 and their probiotic activity against infection by enteropathogenic E. coli (EPEC. 104 intestinal E. coli isolates from domestic pigs were tested by PCR for the occurrence of virulence-associated genes, genes coding for resistances to antimicrobial agents and metals, and for phylogenetic origin by PCR. Adhesion rates and probiotic activity were examined for correlation with the presence of these genes. Finally, data were compared with those from 93 E. coli isolates from wild boars. Isolates from domestic pigs carried a broad variety of all tested genes and showed great diversity in gene patterns. Adhesions varied with a maximum of 18.3 or 24.2 mean bacteria adherence per epithelial cell after 2 or 6 hours respectively. Most isolates from domestic pigs and wild boars showed low adherence, with no correlation between adhesion/probiotic activity and E. coli genes or gene clusters. The gene sfa/foc, encoding for a subunit of F1C fimbriae did show a positive correlative association with adherence and probiotic activity; however E. coli isolates from wild boars with the sfa/foc gene showed less adhesion and probiotic activity than E. coli with the sfa/foc gene isolated from domestic pigs after 6 hour incubation. In conclusion, screening porcine E. coli for virulence associated genes genes, adhesion to intestinal epithelial cells, and probiotic activity revealed a single important adhesion factor, several probiotic candidates, and showed important differences between E. coli of domestic pigs and wild boars.

  2. High throughput ratio imaging to profile caspase activity: potential application in multiparameter high content apoptosis analysis and drug screening.

    Directory of Open Access Journals (Sweden)

    Jeena Joseph

    Full Text Available Recent advancement in the area of green fluorescent protein techniques coupled with microscopic imaging has significantly contributed in defining and dissecting subcellular changes of apoptosis with high spatio-temporal resolution. Although single cell based studies using EGFP and associated techniques have provided valuable information of initiation and hierarchical changes of apoptosis, they are yet to be exploited for multiparameter cell based real time analysis for possible drug screening or pathway defining in a high throughput manner. Here we have developed multiple cancer cell lines expressing FRET sensors for active caspases and adapted them for high throughput live cell ratio imaging, enabling high content image based multiparameter analysis. Sensitivity of the system to detect live cell caspase activation was substantiated by confocal acceptor bleaching as well as wide field FRET imaging. Multiple caspase-specific activities of DEVDase, IETDase and LEHDase were analysed simultaneously with other decisive events of cell death. Through simultaneous analysis of caspase activation by FRET ratio change coupled with detection of mitochondrial membrane potential loss or superoxide generation, we identified several antitumor agents that induced caspase activation with or without membrane potential loss or superoxide generation. Also, cells that escaped the initial drug-induced caspase activation could be easily followed up for defining long term fate. Employing such a revisit imaging strategy of the same area, we have tracked the caspase surviving fractions with multiple drugs and its subsequent response to retreatment, revealing drug-dependent diverging fate of surviving cells. This thereby indicates towards a complex control of drug induced tumor resistance. The technique described here has wider application in both screening of compound libraries as well as in defining apoptotic pathways by linking multiple signaling to identify non

  3. Combinatorial Screening for Transgenic Yeasts with High Cellulase Activities in Combination with a Tunable Expression System.

    Directory of Open Access Journals (Sweden)

    Yoichiro Ito

    Full Text Available Combinatorial screening used together with a broad library of gene expression cassettes is expected to produce a powerful tool for the optimization of the simultaneous expression of multiple enzymes. Recently, we proposed a highly tunable protein expression system that utilized multiple genome-integrated target genes to fine-tune enzyme expression in yeast cells. This tunable system included a library of expression cassettes each composed of three gene-expression control elements that in different combinations produced a wide range of protein expression levels. In this study, four gene expression cassettes with graded protein expression levels were applied to the expression of three cellulases: cellobiohydrolase 1, cellobiohydrolase 2, and endoglucanase 2. After combinatorial screening for transgenic yeasts simultaneously secreting these three cellulases, we obtained strains with higher cellulase expressions than a strain harboring three cellulase-expression constructs within one high-performance gene expression cassette. These results show that our method will be of broad use throughout the field of metabolic engineering.

  4. Quercetin-loaded PLGA nanoparticles: a highly effective antibacterial agent in vitro and anti-infection application in vivo

    Energy Technology Data Exchange (ETDEWEB)

    Sun, Dongdong; Li, Nuan; Zhang, Weiwei; Yang, Endong; Mou, Zhipeng; Zhao, Zhiwei; Liu, Haiping; Wang, Weiyun, E-mail: weiywswzy@163.com [Anhui Agricultural University, School of Life Sciences (China)

    2016-01-15

    Nanotechnology-based approaches have tremendous potential for enhancing efficacy against infectious diseases. PLGA-based nanoparticles as drug delivery carrier have shown promising potential, owing to their sizes and related unique properties. This article aims to develop nanosized poly (d, l-lactide-co-glycolide) PLGA nanoparticle formulation loaded with quercetin (QT). QT is an antioxidant and antibacterial compound isolated from Chinese traditional medicine with low skin permeability and extreme water insolubility. The quercetin-loaded PLGA nanoparticles (PQTs) were synthesized by emulsion–solvent evaporation method and stabilized by coating with poly (vinyl alcohol). The characteristics of PQTs were analyzed by Fourier transform infrared spectroscopy, Ultraviolet–Visible spectroscopy, scanning electron microscope, transmission electron microscopy, and atomic force microscopy, respectively. The PQTs showed a spherical shape with an average size of 100–150 nm. We compared the antibacterial effects of PQTs against Escherichia coli (E. coli) and Micrococcus tetragenus (M. tetragenus).The PQTs produced stronger antibacterial activity to E. coli than that to M. tetragenus through disrupting bacterial cell wall integrity. The antibacterial ratio was increased with the increasing dosages and incubation time. Next, we tested the in vivo antibacterial activity in mice. No noticeable organ damage was captured from H&E-staining organ slices, suggesting the promise of using PQTs for in vivo applications. The results of this study demonstrated the interaction between bacteria and PLGA-based nanoparticles, providing encouragement for conducting further investigations on properties and antimicrobial activity of the PQTs in clinical application.

  5. A multi-assay screening approach for assessment of endocrine-active contaminants in wastewater effluent samples

    International Nuclear Information System (INIS)

    Environmental agencies must monitor an ever increasing range of contaminants of emerging concern, including endocrine disrupting compounds (EDCs). An alternative to using ultra-trace chemical analysis of samples for EDCs is to test for biological activity using in vitro screening assays, then use these assay results to direct analytical chemistry approaches. In this study, we used both analytical approaches and in vitro bioassays to characterize the EDCs present in treated wastewater from four wastewater treatment plants (WWTPs) in Ontario, Canada. Estrogen-mediated activity was assessed using a yeast estrogenicity screening (YES) assay. An in vitro competitive binding assay was used to assess capacity to interfere with binding of the thyroid hormone, thyroxine (T4) to the recombinant human thyroid hormone transport protein, transthyretin (i.e. hTTR). An in vitro binding assay with a rat peroxisome proliferator responsive element transfected into a rainbow trout gill cell line was used to evaluate binding and subsequent gene expression via the peroxisome proliferator activated receptor (PPAR). Analyses of a suite of contaminants known to be EDCs in extracts from treated wastewater were conducted using either gas chromatography with mass spectrometry (GC-MS) or liquid chromatography with tandem mass spectrometry (LC-MS/MS). Estrogenic activity was detected in the YES assay only in those extracts that contained detectable amounts of estradiol (E2). There was a positive relationship between the degree of response in the T4-hTTR assay and the amounts of polybrominated diphenyl ether (PBDE) congeners 47 and 99, triclosan and the PBDE metabolite, 4-OH-BDE17. Several wastewater extracts gave a positive response in the PPAR assay, but these responses were not correlated with the amounts of any of the EDCs analyzed by LC-MS/MS. Overall, these data indicate that a step-wise approach is feasible using a combination of in vitro testing and instrumental analysis to monitor for

  6. A multi-assay screening approach for assessment of endocrine-active contaminants in wastewater effluent samples

    Energy Technology Data Exchange (ETDEWEB)

    Metcalfe, Chris D., E-mail: cmetcalfe@trentu.ca [Environmental and Resource Studies, Trent University, Peterborough, ON, K9J 7B8 (Canada); Kleywegt, Sonya [Standards Development Branch, Ontario Ministry of the Environment, 40 St. Clair Ave. West, Toronto, ON, M4V 1M2 (Canada); Letcher, Robert J. [Ecotoxicology and Wildlife Health Division, Science and Technology Branch, Environment Canada, National Wildlife Research Centre, Carleton University, Ottawa, ON, K1A 0H3 (Canada); Topp, Edward [Agriculture and Agri-Food Canada, Southern Crop Protection and Food Research Centre, London, ON, N5V 7T3 (Canada); Wagh, Purva; Trudeau, Vance L.; Moon, Thomas W. [Department of Biology and Centre for Advanced Research in Environmental Genomics, University of Ottawa, Ottawa, ON, K1N 6N5 (Canada)

    2013-06-01

    Environmental agencies must monitor an ever increasing range of contaminants of emerging concern, including endocrine disrupting compounds (EDCs). An alternative to using ultra-trace chemical analysis of samples for EDCs is to test for biological activity using in vitro screening assays, then use these assay results to direct analytical chemistry approaches. In this study, we used both analytical approaches and in vitro bioassays to characterize the EDCs present in treated wastewater from four wastewater treatment plants (WWTPs) in Ontario, Canada. Estrogen-mediated activity was assessed using a yeast estrogenicity screening (YES) assay. An in vitro competitive binding assay was used to assess capacity to interfere with binding of the thyroid hormone, thyroxine (T4) to the recombinant human thyroid hormone transport protein, transthyretin (i.e. hTTR). An in vitro binding assay with a rat peroxisome proliferator responsive element transfected into a rainbow trout gill cell line was used to evaluate binding and subsequent gene expression via the peroxisome proliferator activated receptor (PPAR). Analyses of a suite of contaminants known to be EDCs in extracts from treated wastewater were conducted using either gas chromatography with mass spectrometry (GC-MS) or liquid chromatography with tandem mass spectrometry (LC-MS/MS). Estrogenic activity was detected in the YES assay only in those extracts that contained detectable amounts of estradiol (E2). There was a positive relationship between the degree of response in the T4-hTTR assay and the amounts of polybrominated diphenyl ether (PBDE) congeners 47 and 99, triclosan and the PBDE metabolite, 4-OH-BDE17. Several wastewater extracts gave a positive response in the PPAR assay, but these responses were not correlated with the amounts of any of the EDCs analyzed by LC-MS/MS. Overall, these data indicate that a step-wise approach is feasible using a combination of in vitro testing and instrumental analysis to monitor for

  7. School Term vs. School Holiday: Associations with Children’s Physical Activity, Screen-Time, Diet and Sleep

    Directory of Open Access Journals (Sweden)

    Amanda E. Staiano

    2015-07-01

    Full Text Available This cross-sectional study examined differences in children’s health behaviors during school term (ST versus school holiday (SH: June–July and how associations changed when weather characteristics were considered. Children aged 5–18 years (n = 406 from a subtropical climate reported behaviors over 20 months. Multivariable regression models controlling for age, sex, race and body mass index z-score(BMIz ) were used to examine associations between SH and each behavior. A second model included heat index, precipitation and daylight hours. Strenuous activity, moderate activity, total activity and TV viewing were significantly higher during SH than ST. After adjusting for weather characteristics, total activity remained significantly higher during SH, but the association with TV viewing was attenuated. Youth surveyed during high precipitation were significantly less likely to meet physical activity guidelines. There were no significant associations between SH and meeting sleep, physical activity or screen-time guidelines. Weather characteristics influenced associations between SH and youth’s physical activity and TV viewing.

  8. Synthetic Lethality Screen Identifies RPS6KA2 as Modifier of Epidermal Growth Factor Receptor Activity in Pancreatic Cancer

    Directory of Open Access Journals (Sweden)

    Nada Milosevic

    2013-12-01

    Full Text Available Pancreatic cancer is characterized by a high degree of resistance to chemotherapy. Epidermal growth factor receptor (EGFR inhibition using the small-molecule inhibitor erlotinib was shown to provide a small survival benefit in a subgroup of patients. To identify kinases whose inhibition acts synergistically with erlotinib, we employed a kinome-wide small-interfering RNA (siRNA-based loss-of-function screen in the presence of erlotinib. Of 779 tested kinases, we identified several targets whose inhibition acted synergistically lethal with EGFR inhibition by erlotinib, among them the S6 kinase ribosomal protein S6 kinase 2 (RPS6KA2/ribosomal S6 kinase 3. Activated RPS6KA2 was expressed in approximately 40% of 123 human pancreatic cancer tissues. RPS6KA2 was shown to act downstream of EGFR/RAS/mitogen-activated protein kinase kinase (MEK/extracellular-signal regulated kinase (ERK signaling and was activated by EGF independently of the presence of KRAS mutations. Knockdown of RPS6KA2 by siRNA led to increased apoptosis only in the presence of erlotinib, whereas RPS6KA2 activation or overexpression rescued from erlotinib- and gemcitabine-induced apoptosis. This effect was at least in part mediated by downstream activation of ribosomal protein S6. Genetic as well as pharmacological inhibition of RPS6KA2 by the inhibitor BI-D1870 acted synergistically with erlotinib. By applying this synergistic lethality screen using a kinome-wide RNA interference-library approach, we identified RPS6KA2 as potential drug target whose inhibition synergistically enhanced the effect of erlotinib on tumor cell survival. This kinase therefore represents a promising drug candidate suitable for the development of novel inhibitors for pancreatic cancer therapy.

  9. Functionalized Carbon Quantum Dots with Dopamine for Tyrosinase Activity Monitoring and Inhibitor Screening: In Vitro and Intracellular Investigation.

    Science.gov (United States)

    Chai, Lujing; Zhou, Jin; Feng, Hui; Tang, Cong; Huang, Yuanyuan; Qian, Zhaosheng

    2015-10-28

    Sensitive assay of tyrosinase (TYR) activity is in urgent demand for both fundamental research and practical application, but the exploration of functional materials with good biocompatibility for its activity evaluation at the intracellular level is still challenging until now. In this work, we develop a convenient and real-time assay with high sensitivity for TYR activity/level monitoring and its inhibitor screening based on biocompatible dopamine functionalized carbon quantum dots (Dopa-CQDs). Dopamine with redox property was functionalized on the surface of carbon quantum dots to construct a Dopa-CQDs conjugate with strong bluish green fluorescence. When the dopamine moiety in Dopa-CQDs conjugate was oxidized to a dopaquinone derivative under specific catalysis of TYR, an intraparticle photoinduced electron transfer (PET) process between CQDs and dopaquinone moiety took place, and then the fluorescence of the conjugate could be quenched simultaneously. Quantitative evaluation of TYR activity was established in terms of the relationship between fluorescence quenching efficiency and TYR activity. The assay covered a broad linear range of up to 800 U/L with a low detection limit of 7.0 U/L. Arbutin, a typical inhibitor of TYR, was chosen as an example to assess its function of inhibitor screening, and positive results were observed that fluorescence quenching extent of the probe was reduced in the presence of arbutin. It is also demonstrated that Dopa-CQD conjugate possesses excellent biocompatibility, and can sensitively monitor intracellular tyrosinase level in melanoma cells and intracellular pH changes in living cells, which provides great potential in application of TYR/pH-associated disease monitoring and medical diagnostics. PMID:26440479

  10. Phytochemical screening and free radical scavenging activity of Citrullus colocynthis seeds extracts

    Directory of Open Access Journals (Sweden)

    Nabila Benariba

    2013-01-01

    Conclusions: These qualitative and quantitative analytical data document the presence in C. colocynthis extracts of such chemical compounds as flavonoids responsible for the antioxidant activity, as well as other biological activities of this plant.

  11. Bioactivity of marine organisms. Part 3. Screening of marine algae of Indian coast for biological activity

    Digital Repository Service at National Institute of Oceanography (India)

    Kamat, S.Y.; Wahidullah, S.; Naik, C.G.; DeSouza, L.; Jayasree, V.; Ambiye, V.; Bhakuni, D.S.; Goel, A.K.; Garg, H.S.; Srimal, R.C.

    Ethanolic extracts from Indian marine algae have been tested for anti-viral, anti-bacterial, anti-fungal, anti-fertility, hypoglycaemic and a wide range of pharmacological activities. Of 34 species investigated 17 appeared biologically active. Six...

  12. Screening for active small molecules in mitochondrial complex I deficient patient's fibroblasts, reveals AICAR as the most beneficial compound.

    Directory of Open Access Journals (Sweden)

    Anna Golubitzky

    Full Text Available Congenital deficiency of the mitochondrial respiratory chain complex I (CI is a common defect of oxidative phosphorylation (OXPHOS. Despite major advances in the biochemical and molecular diagnostics and the deciphering of CI structure, function assembly and pathomechanism, there is currently no satisfactory cure for patients with mitochondrial complex I defects. Small molecules provide one feasible therapeutic option, however their use has not been systematically evaluated using a standardized experimental system. In order to evaluate potentially therapeutic compounds, we set up a relatively simple system measuring different parameters using only a small amount of patient's fibroblasts, in glucose free medium, where growth is highly OXPOS dependent. Ten different compounds were screened using fibroblasts derived from seven CI patients, harboring different mutations.5-Aminoimidazole-4-carboxamide ribotide (AICAR was found to be the most beneficial compound improving growth and ATP content while decreasing ROS production. AICAR also increased mitochondrial biogenesis without altering mitochondrial membrane potential (Δψ. Fluorescence microscopy data supported increased mitochondrial biogenesis and activation of the AMP activated protein kinase (AMPK. Other compounds such as; bezafibrate and oltipraz were rated as favorable while polyphenolic phytochemicals (resverastrol, grape seed extract, genistein and epigallocatechin gallate were found not significant or detrimental. Although the results have to be verified by more thorough investigation of additional OXPHOS parameters, preliminary rapid screening of potential therapeutic compounds in individual patient's fibroblasts could direct and advance personalized medical treatment.

  13. Use of activity-based probes to develop high throughput screening assays that can be performed in complex cell extracts.

    Directory of Open Access Journals (Sweden)

    Edgar Deu

    Full Text Available BACKGROUND: High throughput screening (HTS is one of the primary tools used to identify novel enzyme inhibitors. However, its applicability is generally restricted to targets that can either be expressed recombinantly or purified in large quantities. METHODOLOGY AND PRINCIPAL FINDINGS: Here, we described a method to use activity-based probes (ABPs to identify substrates that are sufficiently selective to allow HTS in complex biological samples. Because ABPs label their target enzymes through the formation of a permanent covalent bond, we can correlate labeling of target enzymes in a complex mixture with inhibition of turnover of a substrate in that same mixture. Thus, substrate specificity can be determined and substrates with sufficiently high selectivity for HTS can be identified. In this study, we demonstrate this method by using an ABP for dipeptidyl aminopeptidases to identify (Pro-Arg2-Rhodamine as a specific substrate for DPAP1 in Plasmodium falciparum lysates and Cathepsin C in rat liver extracts. We then used this substrate to develop highly sensitive HTS assays (Z'>0.8 that are suitable for use in screening large collections of small molecules (i.e >300,000 for inhibitors of these proteases. Finally, we demonstrate that it is possible to use broad-spectrum ABPs to identify target-specific substrates. CONCLUSIONS: We believe that this approach will have value for many enzymatic systems where access to large amounts of active enzyme is problematic.

  14. A high-content EMT screen identifies multiple receptor tyrosine kinase inhibitors with activity on TGFβ receptor

    Science.gov (United States)

    Ackerknecht, Sabine; Lehembre, François; Fink, Tobias; Stritt, Manuel; Wirth, Matthias; Pavan, Simona; Bill, Ruben; Regenass, Urs; Christofori, Gerhard; Meyer-Schaller, Nathalie

    2016-01-01

    An epithelial to mesenchymal transition (EMT) enables epithelial tumor cells to break out of the primary tumor mass and to metastasize. Understanding the molecular mechanisms driving EMT in more detail will provide important tools to interfere with the metastatic process. To identify pharmacological modulators and druggable targets of EMT, we have established a novel multi-parameter, high-content, microscopy-based assay and screened chemical compounds with activities against known targets. Out of 3423 compounds, we have identified 19 drugs that block transforming growth factor beta (TGFβ)-induced EMT in normal murine mammary gland epithelial cells (NMuMG). The active compounds include inhibitors against TGFβ receptors (TGFBR), Rho-associated protein kinases (ROCK), myosin II, SRC kinase and uridine analogues. Among the EMT-repressing compounds, we identified a group of inhibitors targeting multiple receptor tyrosine kinases, and biochemical profiling of these multi-kinase inhibitors reveals TGFBR as a thus far unknown target of their inhibitory spectrum. These findings demonstrate the feasibility of a multi-parameter, high-content microscopy screen to identify modulators and druggable targets of EMT. Moreover, the newly discovered “off-target” effects of several receptor tyrosine kinase inhibitors have important consequences for in vitro and in vivo studies and might beneficially contribute to the therapeutic effects observed in vivo. PMID:27036020

  15. RNA interference screening of interferon-stimulated genes with antiviral activities against classical swine fever virus using a reporter virus.

    Science.gov (United States)

    Wang, Xiao; Li, Yongfeng; Li, Lian-Feng; Shen, Liang; Zhang, Lingkai; Yu, Jiahui; Luo, Yuzi; Sun, Yuan; Li, Su; Qiu, Hua-Ji

    2016-04-01

    Classical swine fever (CSF) caused by classical swine fever virus (CSFV) is a highly contagious and often fatal disease of pigs, which leads to significant economic losses in many countries. Viral infection can induce the production of interferons (IFNs), giving rise to the transcription of hundreds of IFN-stimulated genes (ISGs) to exert antiviral effects. Although numerous ISGs have been identified to possess antiviral activities against different viruses, rare anti-CSFV ISGs have been reported to date. In this study, to screen anti-CSFV ISGs, twenty-one ISGs reported previously were individually knocked down using small interfering RNAs (siRNAs) followed by infection with a reporter CSFV expressing Renilla luciferase (Rluc). As a result, four novel anti-CSFV ISGs were identified, including natural-resistance-associated macrophage protein 1 (NRAMP1), cytosolic 5'-nucleotidase III A (NT5C3A), chemokine C-X-C motif ligand 10 (CXCL10), and 2'-5'-oligoadenylate synthetase 1 (OAS1), which were further verified to exhibit antiviral activities against wild-type CSFV. We conclude that the reporter virus is a useful tool for efficient screening anti-CSFV ISGs.

  16. RNA interference screening of interferon-stimulated genes with antiviral activities against classical swine fever virus using a reporter virus.

    Science.gov (United States)

    Wang, Xiao; Li, Yongfeng; Li, Lian-Feng; Shen, Liang; Zhang, Lingkai; Yu, Jiahui; Luo, Yuzi; Sun, Yuan; Li, Su; Qiu, Hua-Ji

    2016-04-01

    Classical swine fever (CSF) caused by classical swine fever virus (CSFV) is a highly contagious and often fatal disease of pigs, which leads to significant economic losses in many countries. Viral infection can induce the production of interferons (IFNs), giving rise to the transcription of hundreds of IFN-stimulated genes (ISGs) to exert antiviral effects. Although numerous ISGs have been identified to possess antiviral activities against different viruses, rare anti-CSFV ISGs have been reported to date. In this study, to screen anti-CSFV ISGs, twenty-one ISGs reported previously were individually knocked down using small interfering RNAs (siRNAs) followed by infection with a reporter CSFV expressing Renilla luciferase (Rluc). As a result, four novel anti-CSFV ISGs were identified, including natural-resistance-associated macrophage protein 1 (NRAMP1), cytosolic 5'-nucleotidase III A (NT5C3A), chemokine C-X-C motif ligand 10 (CXCL10), and 2'-5'-oligoadenylate synthetase 1 (OAS1), which were further verified to exhibit antiviral activities against wild-type CSFV. We conclude that the reporter virus is a useful tool for efficient screening anti-CSFV ISGs. PMID:26868874

  17. Antimicrobial peptides: mediators of innate immunity as templates for the development of novel anti-infective and immune therapeutics.

    Science.gov (United States)

    Hiemstra, P S; Fernie-King, B A; McMichael, J; Lachmann, P J; Sallenave, J-M

    2004-01-01

    Antimicrobial molecules are ancient and essential small cationic molecules of the host defence system which are found in a wide variety of species. They display antimicrobial activity against a wide range of bacteria, fungi and viruses, an activity that has been mostly attributed to the disruption of microbial membranes. In this article, we will review the "classical" functions of 3 classes of antimicrobial molecules, namely defensins, cathelicidins, and the four-disulfide core proteins secretory leukocyte proteinase inhibitor (SLPI) and elafin. In addition to the study of their expression in a variety of cell types and the regulation of their production, we will also describe novel properties of these molecules that have been highlighted by recent studies. These include their ability to chemoattract a variety of inflammatory, immune and other cell types (neutrophils, macrophages, monocytes, lymphocytes, mast cells, epithelial cells) in vitro and in vivo. In addition, we will discuss the potential use of these newly discovered properties for therapeutic or vaccination purposes, using protein- or gene-transfer based methodologies. Finally, we will examine in an extensive fashion the strategies used by microorganisms to circumvent and subvert host defence mechanisms, such as the modifications of cell membranes and walls, the secretion of inactivating proteins and proteases and the down-regulation of expression of antimicrobial molecules. Increased understanding of the mechanisms used by both the host and the microbes to 'win the battle' may ultimately lead to new therapeutic strategies aimed to treat infectious diseases. PMID:15379675

  18. Antimicrobial peptides: mediators of innate immunity as templates for the development of novel anti-infective and immune therapeutics.

    Science.gov (United States)

    Hiemstra, P S; Fernie-King, B A; McMichael, J; Lachmann, P J; Sallenave, J-M

    2004-01-01

    Antimicrobial molecules are ancient and essential small cationic molecules of the host defence system which are found in a wide variety of species. They display antimicrobial activity against a wide range of bacteria, fungi and viruses, an activity that has been mostly attributed to the disruption of microbial membranes. In this article, we will review the "classical" functions of 3 classes of antimicrobial molecules, namely defensins, cathelicidins, and the four-disulfide core proteins secretory leukocyte proteinase inhibitor (SLPI) and elafin. In addition to the study of their expression in a variety of cell types and the regulation of their production, we will also describe novel properties of these molecules that have been highlighted by recent studies. These include their ability to chemoattract a variety of inflammatory, immune and other cell types (neutrophils, macrophages, monocytes, lymphocytes, mast cells, epithelial cells) in vitro and in vivo. In addition, we will discuss the potential use of these newly discovered properties for therapeutic or vaccination purposes, using protein- or gene-transfer based methodologies. Finally, we will examine in an extensive fashion the strategies used by microorganisms to circumvent and subvert host defence mechanisms, such as the modifications of cell membranes and walls, the secretion of inactivating proteins and proteases and the down-regulation of expression of antimicrobial molecules. Increased understanding of the mechanisms used by both the host and the microbes to 'win the battle' may ultimately lead to new therapeutic strategies aimed to treat infectious diseases.

  19. Screening for lipid yielding microalgae: activities for 1983. Final subcontract report

    Energy Technology Data Exchange (ETDEWEB)

    Thomas, W. H.; Tornabene, T. G.; Weissman, J.

    1984-04-01

    The SERI/DOE Aquatic Species Program is conducting a screening project, to select microalgae species and strains that are acceptable for liquid fuel production in outdoor culture. The emphases are on finding species that grow rapidly at high biomass density, in outdoor culture and produce large quantities of lipids. During 1983 over 100 species were isolated from saline waters at the California and Nevada deserts. Some of these species were characterized for growth response to various nutrients, temperatures, and salinities. Selected species were analyzed for lipid composition. Lipids were characterized into fractions, hydrocarbons, isoprenoids, triglyceride, glycolipids, and phospholipids. The most promising species were tested for growth and monoculture sustainability in outdoor culture. Each section (microalgae selection, chemical profiles of microalgae, mass culture of macroalgae) was abstracted separately. 51 references, 8 figures, 14 tables.

  20. A Genetic Screen Identifies PITX1 as a Suppressor of RAS Activity and Tumorigenicity

    NARCIS (Netherlands)

    Kolfschoten, I.G.M.; Leeuwen, Bart van; Berns, K.; Mullenders, J.; Beijersbergen, R.L.; Bernards, R.A.; Voorhoeve, P.M.; Agami, R.

    2005-01-01

    Activating mutations of RAS frequently occur in subsets of human cancers, indicating that RAS activation is important for tumorigenesis. However, a large proportion of these cancers still retain wild-type RAS alleles, suggesting that either the RAS pathway is activated in a distinct manner or anothe

  1. Improving pharmacokinetic-pharmacodynamic modeling to investigate anti-infective chemotherapy with application to the current generation of antimalarial drugs.

    Directory of Open Access Journals (Sweden)

    Katherine Kay

    Full Text Available Mechanism-based pharmacokinetic-pharmacodynamic (PK/PD modelling is the standard computational technique for simulating drug treatment of infectious diseases with the potential to enhance our understanding of drug treatment outcomes, drug deployment strategies, and dosing regimens. Standard methodologies assume only a single drug is used, it acts only in its unconverted form, and that oral drugs are instantaneously absorbed across the gut wall to their site of action. For drugs with short half-lives, this absorption period accounts for a significant period of their time in the body. Treatment of infectious diseases often uses combination therapies, so we refined and substantially extended the PK/PD methodologies to incorporate (i time lags and drug concentration profiles resulting from absorption across the gut wall and, if required, conversion to another active form; (ii multiple drugs within a treatment combination; (iii differing modes of action of drugs in the combination: additive, synergistic, antagonistic; (iv drugs converted to an active metabolite with a similar mode of action. This methodology was applied to a case study of two first-line malaria treatments based on artemisinin combination therapies (ACTs, artemether-lumefantrine and artesunate-mefloquine where the likelihood of increased artemisinin tolerance/resistance has led to speculation on their continued long-term effectiveness. We note previous estimates of artemisinin kill rate were underestimated by a factor of seven, both the unconverted and converted form of the artemisinins kill parasites and the extended PK/PD methodology produced results consistent with field observations. The simulations predict that a potentially rapid decline in ACT effectiveness is likely to occur as artemisinin resistance spreads, emphasising the importance of containing the spread of artemisinin resistance before it results in widespread drug failure. We found that PK/PD data is generally very

  2. Screening the antiangiogenic activity of medicinal plants grown and sold in Jordan.

    Science.gov (United States)

    Zihlif, Malek; Afifi, Fatma; Muhtaseb, Ruba; Al-Khatib, Sondos; Abaza, Ismail; Naffa, Randa

    2012-02-01

    Angiogenesis is essential for the growth, invasion, and metastasis of most solid tumors and has become a valuable pharmacological target for cancer prevention and treatment. This study was performed to assess the antiangiogenic activity of 31 medicinal plants grown and sold in Jordan. The antiangiogenic activity was assessed using the rat aortic ring assay. Out of 31 extracts, 15 extracts showed more than 50 % inhibition of the blood vessels outgrowth from the primary tissue explants (p = 0.000). Three of these 15 extracts showed a potential cytotoxic effect on normal fibroblast cells. Four extracts shared antiangiogenic and antiproliferative activity towards MCF7 breast cancer cell lines. Eight extracts demonstrated selective antiangiogenic activity. This is the first report demonstrating the potential antiangiogenic activity of Artemisia judaica, Aloysia citriodora, Salvia egyptiaca, and Calendula arvensis. Some extracts with antiangiogenic activity exhibited selectivity against the endothelial cells proliferation, demonstrating a direct inhibitory activity against the key step in tumor angiogenesis. PMID:22174075

  3. A Class of High-affinity Bicyclooctane G551D-CFTR Activators Identified by High Throughput Screening

    Institute of Scientific and Technical Information of China (English)

    HE Cheng-yan; ZHAO Lu; LIU Yan-li; XU Li-na; SHANG De-jing; YANG Hong

    2004-01-01

    The glycine-to-aspartic acid missense mutation at the codon 551(G551D) of the cystic fibrosis transmembrane conductance regulator(CFTR) is one of the five most frequent cystic fibrosis(CF) mutations associated with a severe CF phenotype. To explore the feasibility of pharmacological correction of disrupted activation of CFTR chloride channel caused by G551D mutation, we developed a halide-sensitive fluorescence miniassay for G551D-CFTR in Fisher rat thyroid(FRT) epithelial cells for the discovery of novel activators of G551D-CFTR. A class of bicyclooctane small molecule compounds that efficiently stimulate G551D-CFTR chloride channel activity was identified by high throughput screening via the FRT cell-based assay. This class of compounds selectively activates G551D-CFTR with a high affinity, whereas little effect of the compounds on wildtype CFTR can be seen. The discovery of a class of bicyclooctane G551D-CFTR activators will permit the analysis of structure-activity relationship of the compounds to identify ideal leads for in vivo therapeutic studies.

  4. Identification of β-hematin inhibitors in a high-throughput screening effort reveals scaffolds with in vitro antimalarial activity

    Directory of Open Access Journals (Sweden)

    Rebecca D. Sandlin

    2014-12-01

    Full Text Available The emergence of drug resistant strains of Plasmodium spp. creates a critical need for the development of novel antimalarials. Formation of hemozoin, a crystalline heme detoxification process vital to parasite survival serves as an important drug target. The quinoline antimalarials including chloroquine and amodiaquine owe their antimalarial activity to inhibition of hemozoin formation. Though in vivo formation of hemozoin occurs within the presence of neutral lipids, the lipophilic detergent NP-40 was previously shown to serve as a surrogate in the β-hematin (synthetic hemozoin formation process. Consequently, an NP-40 mediated β-hematin formation assay was developed for use in high-throughput screening. Here, the assay was utilized to screen 144,330 compounds for the identification of inhibitors of crystallization, resulting in 530 hits. To establish the effectiveness of these target-based β-hematin inhibitors against Plasmodium falciparum, each hit was further tested in cultures of parasitized red blood cells. This effort revealed that 171 of the β-hematin inhibitors are also active against the parasite. Dose–response data identified 73 of these β-hematin inhibitors have IC50 values ⩽5 μM, including 25 compounds with nanomolar activity against P. falciparum. A scaffold-based analysis of this data identified 14 primary scaffolds that represent 46% of the 530 total hits. Representative compounds from each of the classes were further assessed for hemozoin inhibitory activity in P. falciparum infected human erythrocytes. Each of the hit compounds tested were found to be positive inhibitors, while a negative control did not perturb this biological pathway in culture.

  5. Coloured cornea replacements with anti-infective properties: expanding the safe use of silver nanoparticles in regenerative medicine

    Science.gov (United States)

    Alarcon, E. I.; Vulesevic, B.; Argawal, A.; Ross, A.; Bejjani, P.; Podrebarac, J.; Ravichandran, R.; Phopase, J.; Suuronen, E. J.; Griffith, M.

    2016-03-01

    Despite the broad anti-microbial and anti-inflammatory properties of silver nanoparticles (AgNPs), their use in bioengineered corneal replacements or bandage contact lenses has been hindered due to their intense yellow coloration. In this communication, we report the development of a new strategy to pre-stabilize and incorporate AgNPs with different colours into collagen matrices for fabrication of corneal implants and lenses, and assessed their in vitro and in vivo activity.Despite the broad anti-microbial and anti-inflammatory properties of silver nanoparticles (AgNPs), their use in bioengineered corneal replacements or bandage contact lenses has been hindered due to their intense yellow coloration. In this communication, we report the development of a new strategy to pre-stabilize and incorporate AgNPs with different colours into collagen matrices for fabrication of corneal implants and lenses, and assessed their in vitro and in vivo activity. Electronic supplementary information (ESI) available: Collagen hydrogel, moulded as a cornea, prepared containing collagen protected AgNPs and representative images for collagen hydrogels, moulded as corneas, containing Blue AgNPs either unprotected or protected with LL37-SH; representative TEM images for Green-1 AgNPs prepared in this work; changes on surface plasmon band after synthesis for Green-2 AgNPs without LL37-SH; representative picture of the powder obtained for Green-1 AgNPs capped with LL37-SH after 72 h lyophilization, see main text; representative TEM images for Blue and Green-1 AgNPs prepared in this work; absorption spectra for the supernatants for collagen hydrogels containing Blue AgNPs; absorbance at 600 nm of PAO1 cultures prepared in 25% LB media incubated for 14 h at 37 °C in the presence of different concentrations of AgNPs, Green-1 or Blue, or silver nitrate; HECC cell density (cells per cm2) measured on gels with and without silver nitrate after 1 day of cell incubation; total silver concentration

  6. Screening of twenty five plant extracts for larvicidal activity against Culex quinquefasciatus Say (Diptera:Culicidae)

    Institute of Scientific and Technical Information of China (English)

    Samuel Tennyson; K John Ravindran; S Arivoli

    2012-01-01

    Objective: To determine the larvicidal activity of twenty five plant extracts against Culex quinquefasciatus (Cx. quinquefasciatus). Methods: The larvicidal activity was determined against the third instar larvae of Cx. quinquefasciatus at 1 000 ppm concentration. Larval mortality was assessed after 24 and 48 h. Results: The hexane extracts of Cleistanthus collinus (C. collinus) and Murraya koeingii (M. koeingii) plants showed 100 percent mortality at 24 h bioassay followed by diethyl ether, dichloromethane and ethyl acetate extracts of C. collinus, Leucas aspera (L. aspera), Hydrocotyle javanica (H. javanica), M. koeingii, Sphaeranthus indicus (S. indicus) and Zanthoxylum limonella (Z. limonella) after 48 h exposure. Conclusions: The results indicate larvicidal activity against Cx. quinquefasciatus and further investigations are needed to elucidate this activity against a wide range of all stages of mosquito species and also the active ingredients of the extract responsible for larvicidal activity should be identified.

  7. Screening of Ficus religiosa leaves fractions for analgesic and anti-inflammatory activities

    OpenAIRE

    Vishal Gulecha; Sivakumar, T.; Aman Upaganlawar; Manoj Mahajan; Chandrashekhar Upasani

    2011-01-01

    Objective : To evaluate the different fractions of dried leaves of Ficus religiosa Linn for analgesic and anti-inflammatory activity using different models of pain and inflammation Materials and Methods : The analgesic activity of F. religiosa carried out using acetic acid-induced writhing in mice and tail flick test in rats. The anti-inflammatory activity was evaluated using carrageenan-induced rat paw edema and cotton pellet-granuloma formation in rats. Five different fractions (FRI, FR...

  8. Biological activity of Aronia melanocarpa antioxidants pre-screening in intervention study design

    OpenAIRE

    Konić-Ristić Aleksandra; Srdić-Rajić Tatjana; Kardum Nevena; Glibetić Marija

    2013-01-01

    Beneficial effects of black chokeberry fruits and juices in health promotion and prevention of chronic diseases shown both in epidemiological and dietary intervention studies are often connected with their antioxidant activity. The aim of this study was to investigate the total phenolics and anthocyanins content, chemical antioxidant activity (DPPH-assay), antioxidant protection in erythrocytes and anti-platelet activity in vitro of three different chokeberry products: commercial and fr...

  9. Obesity, overweight, screen time and physical activity in Mexican adolescents Obesidad, sobrepeso, tiempo frente a la pantalla y actividad física en adolescentes mexicanos

    OpenAIRE

    María del Carmen Morales-Ruán; Bernardo Hernández-Prado; Luz María Gómez-Acosta; Teresa Shamah-Levy; Lucía Cuevas-Nasu

    2009-01-01

    OBJECTIVE: To determine whether screen time and physical activity is related to overweight or obesity in adolescents. MATERIAL AND METHODS: Cross-sectional design. Adolescents aged 10 to 19 were included in the Mexican National Health and Nutrition Survey 2006 (ENSANUT 2006). The dependent variable was overweight or obesity; the independent variable was screen time. A logistic regression model was created to estimate the relationship of overweight and obesity to various factors, including scr...

  10. Active play and screen time in US children aged 4 to 11 years in relation to sociodemographic and weight status characteristics: a nationally representative cross-sectional analysis

    Directory of Open Access Journals (Sweden)

    Must Aviva

    2008-10-01

    Full Text Available Abstract Background The high prevalence of childhood obesity underscores the importance of monitoring population trends in children's activity and screen time, and describing associations with child age, gender, race/ethnicity, and weight status. Our objective was to estimate the proportion of young children in the US who have low levels of active play or high levels of screen time, or who have both these behaviors, and to describe associations with age, gender, race/ethnicity, and weight status. Methods We analyzed data collected during the National Health and Nutrition Examination Surveys 2001–2004, a US nationally representative cross-sectional study. We studied 2964 children aged 4.00 to 11.99 years. Our main outcomes were reported weekly times that the child played or exercised hard enough to sweat or breathe hard (active play, daily hours the child watched television/videos, used computers, or played computer games (screen time, and the combination of low active play and high screen time. Low active play was defined as active play 6 times or less per week. High screen time was defined as more than 2 hours per day. We accounted for the complex survey design in analyses and report proportions and 95% confidence intervals. We used Wald Chi-square to test for differences between proportions. To identify factors associated with low active play and high screen time, we used multivariate logistic regression. Results Of US children aged 4 to 11 years, 37.3% (95% confidence interval, 34.1% to 40.4% had low levels of active play, 65.0% (95% CI, 61.4% to 68.5% had high screen time, and 26.3% (95% CI, 23.8% to 28.9% had both these behaviors. Characteristics associated with a higher probability of simultaneously having low active play and high screen time were older age, female gender, non-Hispanic black race/ethnicity, and having a BMI-for-age ≥95th percentile of the CDC growth reference. Conclusion Many young children in the US are reported to

  11. PRELIMINARY PHYTOCHEMICAL SCREENING OF ANTIBACTERIAL ACTIVITY OF PALMYRA PALM ( BORASSUS FLABELLIFER) ROOT EXTRACT

    OpenAIRE

    Saravanan C., Priya B.*, Asir Bradley S. and Uma Sundaram

    2012-01-01

    The phytochemical constituents of Borassus flabellifer was identified and evaluated the antibacterial activity of the acetone, benzene, chloroform, ethanol and methanol extracts. A phytoconstituent analysis of alkaloids, glycosides, terpenoids, steroids, flavonoids, tannins, phenols and saponins were performed on the various solvent extracts. Antibacterial activity was analyzed by agar well diffusion method against five pathogenic microorganisms, E. coli, S. aureus, K. pneumonia, P. aeruginos...

  12. Screening of African medicinal plants for antimicrobial and enzyme inhibitory activity.

    Science.gov (United States)

    Tshibangu, Jeannette Ndaya; Chifundera, Kusamba; Kaminsky, Ronald; Wright, Anthony David; König, Gabriele Maria

    2002-04-01

    Seven plant species, belonging to different families, were collected in the eastern part of the Republic of Congo (Kivu) based on ethnopharmacological information. Their dichloromethane and methanolic extracts were tested for biological activity. Five of the seven collected plants exhibited antiplasmodial activity with IC(50) values ranging from 1.1 to 9.8 microg/ml. The methanolic extract of Cissampelos mucronata was the most active one showing activity against chloroquine sensitive (D6) and chloroquine resistant (W2) Plasmodium falciparum strains with IC(50) values of 1.5 and 1.1 microg/ml, respectively. Additionally, this extract significantly inhibited the enzyme tyrosine kinase p56(lck) (TK). The dichloromethane extract of Amorphophallus bequaertii inhibited the growth of Mycobacterium tuberculosis with a MIC of 100 microg/ml and the methanolic extract of Rubus rigidus inhibited the activity of both enzymes HIV1-reverse transcriptase (HIV1-RT) and TK p56(lck). PMID:11891084

  13. Screening for antibacterial principle and activity of Aerva javanica (Burm .f) Juss. ex Schult.

    Institute of Scientific and Technical Information of China (English)

    P Srinivas; S Ram Reddy

    2012-01-01

    Objective: To investigate the antibacterial principle and activity of Aerva javanica, a medicinal plant. Methods: Crude extracts of different parts of Aerva javanica were made with hexane, chloroform and methanol. Phytochemical analysis of the crude extracts was done by following the standard methodology, and antibacterial activity was evaluated by inhibition zone and MIC values. Crude extracts were resolved through HPTLC and the antibacterial activity of the separated compounds was evaluated by bioautography. Results: The yields of crude extracts made from different plant parts varied both with plant part and solvent. Methanolic extracts of leaf and flower have shown a wide range of phytochemicals and more antibacterial activity. HPTLC separation of extracts coupled with bioautography studies revealed that apigenin followed by rutin and kaempferol has shown antibacterial activity against more number of bacteria. Conclusions:The present study supports the use of Aerva javanica in the traditional medicine, and it can be used against bacterial infections.

  14. Screening for antimalarial and acetylcholinesterase inhibitory activities of some Iranian seaweeds.

    Science.gov (United States)

    Ghannadi, A; Plubrukarn, A; Zandi, K; Sartavi, K; Yegdaneh, A

    2013-04-01

    Alcoholic extracts of 8 different types of seaweeds from Iran's Persian Gulf were tested for their antimalarial and acetylcholinesterase enzyme (AChE) inhibitory activities for the first time. A modified Ellman and Ingkaninan method was used for measuring AChE inhibitory activity in which galanthamine was used as the reference. The antimalarial assay was performed using microculture radioisotope technique. Mefloquine and dihydroartemisinin were uased as the standards. The extract of Sargassum boveanum (Sargasseae family) showed the highest AChE inhibitory activity (IC50 equals to 1 mg ml(-1)) while Cystoseira indica (Cystoseiraceae family) exhibited the least activity (IC50 of 11 mg ml(-1)). The species from Rhodophyta (Gracilaria corticata and Gracilaria salicornia) also showed moderate activities (IC509.5, 8.7 mg ml(-1), respectively). All extracts were inactive in antimalarial assay. PMID:24019820

  15. Rapid screening of {sup 90}Sr activity in water and milk samples using Cherenkov radiation

    Energy Technology Data Exchange (ETDEWEB)

    Stamoulis, K.C. [Archaeometry Center, University of Ioannina, 45110 Ioannina (Greece)]. E-mail: kstamoul@cc.uoi.gr; Ioannides, K.G. [Archaeometry Center, University of Ioannina, 45110 Ioannina (Greece); Nuclear Physics Laboratory, University of Ioannina, 45110 Ioannina (Greece); Karamanis, D.T. [Nuclear Physics Laboratory, University of Ioannina, 45110 Ioannina (Greece); Patiris, D.C. [Nuclear Physics Laboratory, University of Ioannina, 45110 Ioannina (Greece)

    2007-07-01

    A method for screening {sup 90}Sr in milk samples is proposed. This method is based on a liquid scintillation technique taking advantage of Cherenkov radiation, which is produced in a liquid medium and then detected by the photomultipliers of a Liquid Scintillation Counter (LSC). Twenty millilitres of water and milk samples spiked with various concentrations of {sup 90}Sr/{sup 90}Y in equilibrium were added in plastic vials and then were measured with an LSC (TriCarb 3170 TR/SL). The derived efficiencies were 49% for water samples and 14% for milk samples. The detection limit was 470 mBq L{sup -1} {sup 90}Sr for water, without any pretreatment. Milk contains potassium, which also produces Cherenkov radiation due to the presence of {sup 40}K. For this reason, the interference of {sup 40}K in the measurements of {sup 90}Sr in milk samples was also investigated. The detection limit for milk was 1.7 Bq L{sup -1} {sup 90}Sr.

  16. High-content screening identifies kinase inhibitors that overcome venetoclax resistance in activated CLL cells.

    Science.gov (United States)

    Oppermann, Sina; Ylanko, Jarkko; Shi, Yonghong; Hariharan, Santosh; Oakes, Christopher C; Brauer, Patrick M; Zúñiga-Pflücker, Juan C; Leber, Brian; Spaner, David E; Andrews, David W

    2016-08-18

    Novel agents such as the Bcl-2 inhibitor venetoclax (ABT-199) are changing treatment paradigms for chronic lymphocytic leukemia (CLL) but important problems remain. Although some patients exhibit deep and durable responses to venetoclax as a single agent, other patients harbor subpopulations of resistant leukemia cells that mediate disease recurrence. One hypothesis for the origin of resistance to venetoclax is by kinase-mediated survival signals encountered in proliferation centers that may be unique for individual patients. An in vitro microenvironment model was developed with primary CLL cells that could be incorporated into an automated high-content microscopy-based screen of kinase inhibitors (KIs) to identify agents that may improve venetoclax therapy in a personalized manner. Marked interpatient variability was noted for which KIs were effective; nevertheless, sunitinib was identified as the most common clinically available KI effective in overcoming venetoclax resistance. Examination of the underlying mechanisms indicated that venetoclax resistance may be induced by microenvironmental signals that upregulate antiapoptotic Bcl-xl, Mcl-1, and A1, which can be counteracted more efficiently by sunitinib than by ibrutinib or idelalisib. Although patient-specific drug responses are common, for many patients, combination therapy with sunitinib may significantly improve the therapeutic efficacy of venetoclax. PMID:27297795

  17. The Breast Cancer Screening Program. The first year of activity on the territory of Pomeranian Region

    International Nuclear Information System (INIS)

    Objectives. The Breast Cancer Screening Program (BCSP) has been launched in January 2007. There are 16 Regional Coordinating Centers. The headquarters are located the the Maria Sklodowska-Curie Memorial Cancer Center - Institute of Oncology, in Warsaw. In Poland breast cancer (BC) accounts for a 20.5% morbidity rate and causes 13% of deaths. Women between 50 and 69 years of age make up half of the breast cancer morbidity group. There is a tendency towards an increase in BC morbidity. Of all the 13385 registered in Poland throughout 2005 641 occurred in the Pomeranian Voivodeship. Material and Methods. There are 31 mammography units in the Pomeranian region. Mammography for women between the ages of 50 and 69 is performed free of charge and financed by the governmental health insurance. In 2007 over 57,500 mammographies were performed in the Pomeranian Voivodeship accounting for some 33.1% of all the women eligible for the BCSP. Results. 298 cases of BC were detected. BCSP increased the likelihood of detecting early BC (T1). T1 BCs were detected in 61.1% and were described by radiologists as stages BIRADS 4 and BIRADS 5. Conclusions. The main aim of the BCSP is reducing the coefficient of BC mortality. The results of BCSP confirmed the need for the continuation of such a program. (authors)

  18. Screening of Marine Actinomycetes from Segara Anakan for Natural Pigment and Hydrolytic Activities

    Science.gov (United States)

    Asnani, A.; Ryandini, D.; Suwandri

    2016-02-01

    Marine actinomycetes have become sources of great interest to natural product chemistry due to their new chemical entities and bioactive metabolites. Since April 2010, we have screened actinobacteria from five sites that represent different ecosystems of Segara Anakan lagoon. In this present study we focus on specific isolates, K-2C which covers 1) actinomycetes identification based on morphology observation and 16S rRNA gene; 2) fermentation and isolation of pigment; 3) structure determination of pigment; and 4) hydrolytic enzymes characterization; Methodologies relevant to the studies were implemented accordingly. The results indicated that K-2C was likely Streptomyces fradiae strain RSU15, and the best fermentation medium should contain starch and casein with 21 days of incubation. The isolate has extracellular as well as intracellular pigments. Isolated pigments gave purple color with λmax of 529.00 nm. The pigment was structurally characterized. Interestingly, Streptomyces K-2C was able to produce potential hydrolytic enzymes such as amylase, cellulase, protease, lipase, urease, and nitrate reductase.

  19. Location performance objectives for the NNWSI area-to-location screening activity

    Energy Technology Data Exchange (ETDEWEB)

    Sinnock, S.; Fernandez, J.A.

    1984-01-01

    Fifty-four objectives were identified to guide the screening of the Nevada Research and Development Area of the Nevada Test Site for relatively favorable locations for the disposal of nuclear waste in a mined geologic repository. The objectives were organized as a hierarchy composed of 4 upper-level, 12 middle-level, and 38 lower-level objectives. The four upper-level objectives account for broad national goals to contain and isolate nuclear waste in an environmentally sound and economically acceptable manner. The middle-level objectives correspond to topical categories that logically relate the upper-level objectives to site-specific concerns such as seismicity, sensitive species, and flooding hazards (represented by the lower-level objectives). The relative merits of alternative locations were compared by an application of decision analysis based on standard utility theory. The relative favorabilities of pertinent physical conditions at each alternative location were weighted in relation to the importance of objectives, and summed to produce maps indicating the most and the least favorable locations. Descriptions of the objectives were organized by the hierarchical format; they detail the applicability of each objective to geologic repository siting, previously published siting criteria corresponding to each objective, and the rationale for the weight assigned to each objective, and the pertinent attributes for evaluating locations with respect to each objective. 51 references, 47 figures, 4 tables.

  20. Bacterial and fungal keratitis in Upper Egypt: In vitro screening of enzymes, toxins and antifungal activity

    Directory of Open Access Journals (Sweden)

    Abdullah A Gharamah

    2014-01-01

    Full Text Available Purpose: This work was conducted to study the ability of bacterial and fungal isolates from keratitis cases in Upper Egypt to produce enzymes, toxins, and to test the isolated fungal species sensitivity to some therapeutic agents. Materials and Methods: One hundred and fifteen patients clinically diagnosed to have microbial keratitis were investigated. From these cases, 37 bacterial isolates and 25 fungal isolates were screened for their ability to produce extra-cellular enzymes in solid media. In addition, the ability of fungal isolates to produce mycotoxins and their sensitivity to 4 antifungal agents were tested. Results: Protease, lipase, hemolysins, urease, phosphatase, and catalase were detected respectively in 48.65%, 37.84%, 59.46%, 43.24%, 67.57%, and 100% out of 37 bacterial isolates tested. Out of 25 fungal isolates tested during the present study, 80% were positive for protease, 84% for lipase and urease, 28% for blood hemolysis, and 100% for phosphatase and catalase enzymes. Thirteen fungal isolates were able to produce detectable amounts of 7 mycotoxins in culture medium (aflatoxins (B1, B2, G1, and G2, sterigmatocystin, fumagillin, diacetoxyscirpenol, zearalenone, T-2 toxin, and trichodermin. Among the antifungal agents tested in this study, terbinafine showed the highest effect against most isolates in vitro. Conclusion: In conclusion, the ability of bacterial and fungal isolates to produce extracellular enzymes and toxins may be aid in the invasion and destruction of eye tissues, which, in turn, lead to vision loss.

  1. Location performance objectives for the NNWSI area-to-location screening activity

    International Nuclear Information System (INIS)

    Fifty-four objectives were identified to guide the screening of the Nevada Research and Development Area of the Nevada Test Site for relatively favorable locations for the disposal of nuclear waste in a mined geologic repository. The objectives were organized as a hierarchy composed of 4 upper-level, 12 middle-level, and 38 lower-level objectives. The four upper-level objectives account for broad national goals to contain and isolate nuclear waste in an environmentally sound and economically acceptable manner. The middle-level objectives correspond to topical categories that logically relate the upper-level objectives to site-specific concerns such as seismicity, sensitive species, and flooding hazards (represented by the lower-level objectives). The relative merits of alternative locations were compared by an application of decision analysis based on standard utility theory. The relative favorabilities of pertinent physical conditions at each alternative location were weighted in relation to the importance of objectives, and summed to produce maps indicating the most and the least favorable locations. Descriptions of the objectives were organized by the hierarchical format; they detail the applicability of each objective to geologic repository siting, previously published siting criteria corresponding to each objective, and the rationale for the weight assigned to each objective, and the pertinent attributes for evaluating locations with respect to each objective. 51 references, 47 figures, 4 tables

  2. Screening of the anticonvulsant activity of some plants from Fabaceae family in experimental seizure models in mice

    Directory of Open Access Journals (Sweden)

    S Sardari

    2011-10-01

    Full Text Available "n  Background and purpose of the study: Fabaceae is the third largest family of flowering plants. Lack of essential oils in the plants of this family can be an advantage in search for safe and effective medicines. In this study the anticonvulsant effect of the leaves of Albizzia julibrissin, Acacia juliflora, Acacia nubica and aerial parts of Astragalus obtusifolius was evaluated in pentylenetetrazole (PTZ and maximal electroshock (MES seizure tests. "n  Methods: The hydroalcoholic extracts of the plants were obtained by percolation. Different doses of the extracts were injected to the mice intraperitoneally (i.p. and occurrence of clonic seizures induced by PTZ (60 mg/kg, i.p. or tonic seizures induced by MES (50 mA, 50Hz, 1sec were monitored up to 30 min after administration. Acute toxicity of the extracts was also assessed. The safe and effective extract was then fractionated by dichloromethane and anticonvulsant activity of the fractions was determined. Finally, the constituents of the extract and the fractions were screened by thin layer chromatography. "n  Results: Among the extracts, only A. obtusifolius extract showed low toxicity and protective effect against clonic seizures with ED50 value of 3.97 g/kg. Fractionation of the extract led to increase in anticonvulsant activity and ED50 value of 2.86 g/kg was obtained for the aqueous fraction. Phytochemical screening revealed the presence of alkaloids, flavonoids, anthrones and saponins in the aqueous fraction. "n  Major conclusion: The presence of anticonvulsant compounds in A. obtusifolius suggests further activity-guided fractionation and analytical studies to find out the potential of this plant as a source of anticonvulsant agent.

  3. Screening of marine bacteria with bacteriocin-like activities and probiotic potential for ornate spiny lobster (Panulirus ornatus) juveniles.

    Science.gov (United States)

    Nguyen, Van Duy; Pham, Thu Thuy; Nguyen, Thi Hai Thanh; Nguyen, Thi Thanh Xuan; Hoj, Lone

    2014-09-01

    Bacteriocins are ribosomally synthesized antimicrobial peptides, which have been found in diverse bacterial species of terrestrial origins and some from the sea. New bacteriocins with new characteristics, new origins and new applications are likely still awaiting discovery. The present study screened bacteria isolated from marine animals of interest to the aquaculture industry for antimicrobial and bacteriocin-like activities in order to uncover biodiversity of bacteriocin producers, and explore the potential application in aquaculture. In total, 24 of 100 screened isolates showed antimicrobial activities and 7 of these exerted bacteriocin-like activities. Sequencing of 16S rRNA genes identified the isolates as members of the six genera Proteus, Providencia, Klebsiella, Alcaligenes, Bacillus and Enterococcus. In some cases, further analysis of housekeeping genes, rpoB for Proteus and recA for Klebsiella, as well as biochemical tests was necessary for identification to species level, and some of the Proteus isolates may represent novel species. The seven bacteriocinogenic isolates showed a wide antimicrobial spectrum against foodborne and animal pathogens, which opens the way to their potential use as marine drugs and probiotics in food, aquaculture, livestock and clinical settings. As a case study, the protective effect of shortlisted bacteriocinogenic isolates were tested in aquaculture-raised spiny lobster (Panulirus ornatus) juveniles. A single-strain (Bacillus pumilus B3.10.2B) and a three-strain (B. pumilus B3.10.2B, Bacillus cereus D9, Lactobacillus plantarum T13) probiotic preparation were added to the feed of Panulirus ornatus juveniles, which were subsequently challenged with the pathogen Vibrio owensii DY05. Juveniles in the probiotic treatments displayed increased growth and reduced feed conversion rates after 60 days, and increased survival rate after pathogen challenge relative to the control. This study represents the first evidence of bacteriocin

  4. Screening of Dengue virus antiviral activity of marine seaweeds by an in situ enzyme-linked immunosorbent assay.

    Directory of Open Access Journals (Sweden)

    Andrea Cristine Koishi

    Full Text Available Dengue is a significant public health problem worldwide. Despite the important social and clinical impact, there is no vaccine or specific antiviral therapy for prevention and treatment of dengue virus (DENV infection. Considering the above, drug discovery research for dengue is of utmost importance; in addition natural marine products provide diverse and novel chemical structures with potent biological activities that must be evaluated. In this study we propose a target-free approach for dengue drug discovery based on a novel, rapid, and economic in situ enzyme-linked immunosorbent assay and the screening of a panel of marine seaweed extracts. The in situ ELISA was standardized and validated for Huh7.5 cell line infected with all four serotypes of DENV, among them clinical isolates and a laboratory strain. Statistical analysis showed an average S/B of 7.2 and Z-factor of 0.62, demonstrating assay consistency and reliability. A panel of fifteen seaweed extracts was then screened at the maximum non-toxic dose previously determined by the MTT and Neutral Red cytotoxic assays. Eight seaweed extracts were able to reduce DENV infection of at least one serotype tested. Four extracts (Phaeophyta: Canistrocarpus cervicornis, Padina gymnospora; Rhodophyta: Palisada perforate; Chlorophyta: Caulerpa racemosa were chosen for further evaluation, and time of addition studies point that they might act at an early stage of the viral infection cycle, such as binding or internalization.

  5. High content screening of a kinase-focused library reveals compounds broadly-active against dengue viruses.

    Directory of Open Access Journals (Sweden)

    Deu John M Cruz

    Full Text Available Dengue virus is a mosquito-borne flavivirus that has a large impact in global health. It is considered as one of the medically important arboviruses, and developing a preventive or therapeutic solution remains a top priority in the medical and scientific community. Drug discovery programs for potential dengue antivirals have increased dramatically over the last decade, largely in part to the introduction of high-throughput assays. In this study, we have developed an image-based dengue high-throughput/high-content assay (HT/HCA using an innovative computer vision approach to screen a kinase-focused library for anti-dengue compounds. Using this dengue HT/HCA, we identified a group of compounds with a 4-(1-aminoethyl-N-methylthiazol-2-amine as a common core structure that inhibits dengue viral infection in a human liver-derived cell line (Huh-7.5 cells. Compounds CND1201, CND1203 and CND1243 exhibited strong antiviral activities against all four dengue serotypes. Plaque reduction and time-of-addition assays suggests that these compounds interfere with the late stage of viral infection cycle. These findings demonstrate that our image-based dengue HT/HCA is a reliable tool that can be used to screen various chemical libraries for potential dengue antiviral candidates.

  6. Screening of biological activities of Polygonum maritimum L. from Algerian coast

    Institute of Scientific and Technical Information of China (English)

    Imad Abdelhamid El-Haci; Fawzia Atik Bekkara; Wissame Mazari; Fayal Hassani; Mohamed Amine Didi

    2013-01-01

    Objective: To investigate the antioxidant and the antibacterial activities of crude extract from aerial part of Polygonum maritimum L. (Polygonaceae) (P. maritimum) and to find new actives biomolecules. Methods:The whole plant was collected from the Rechgoune coast (West of Algeria), and methanolic crude extract of aerial parts of P. maritimum (PMCE) was prepared. The extract was tested against different bacterial strain and tested for his ability to neutralize free radical (DPPH) and to scavenge the H2O2. Results:PMCE had a very high content of total phenol, which was (352.49±18.03) mg/g dry weight,expressed as gallic acid equivalent. PMCE exhibited excellent antioxidant activity, as measured using DPPH and H2O2 scavenging assays. It also showed a high antibacterial activity against gram-positive bacterial strains: Bacillus cereus, Bacillus subtilis and Staphylococcus aureus with an highest MIC of 120 µg/mL. Conclusions: The antioxidant and antibacterial activity of the PMCE is probably due to phenolic compounds present in the extract. The contemporary presence of antioxidant and antibacterial activities in the PMCE suggests that this plant may be a source of bioactive substances with multifaceted activity.

  7. In vitro screening of 1-aryl-6-hydroxy-1,2,3,4-tetrahydroisoquinolines: structure related activity against pathogenic bacteria

    Institute of Scientific and Technical Information of China (English)

    Moses; Njutain; Ngemenya; Joelle; Ngo; Hanna; Julios; Armand; Komtchou; Simon; Mbua; Ngale; Efange

    2015-01-01

    Objective: To evaluate the antibacterial activity of ten synthetic tetrahydroisoquinolines against eight bacterial strains. Methods: The ten tetrahydroisoquinolines synthesized via base-catalyzed Pictet-Spengler cyclization were screened against a total of eight bacterial strains comprising control and pathogenic strains by the disc diffusion and micro-dilution methods. The most active compound was then assessed for cytotoxicity on human lymphocytes. Results: Six of the tetrahydroisoquinolines showed broad spectrum bacteriostatic activity. The zones of inhibition produced ranged from 7 to 23 mm for 200 μg per disc. The presence of a lipophilic substituent at the para position of the pendant phenyl group conferred the highest antibacterial activity. Compound 2 [1-(3,4-chlorophenyl)-6-hydroxy-1,2,3,4-tetrahydroisoquinoline] was the most active and produced zones ranging from 9 to 20 mm against all eight bacterial strains. Compound 2 also showed the lowest minimum inhibitory concentration of 100 μg/mL against Escherichia coli ATCC11775 and the lowest minimum bactericidal concentration of 800 μg/mL against pathogenic Salmonella typhimurium. Overall, compound 2 was the most active with bacteriostatic and bactericidal activity against three and four bacterial strains respectively. A 50% cytotoxic concentration of 98.2 μg/mL was recorded for compound 2 indicating a low risk of toxicity. Conclusions: The 1-aryl-1,2,3,4-tetrahydroisoquinolines display structure-related antibacterial activity and further chemical exploration of the tetrahydroisoquinoline scaf old may yield more potent non-toxic derivatives for development into new antibacterials.

  8. Pharmacological screening of Hypericum androsaemum extracts for antioxidant, anti-lipid peroxidation, antiglycation and cytotoxicity activity.

    Science.gov (United States)

    Saddiqe, Zeb; Maimoona, Alya; Abbas, Ghulam; Naeem, Ismat; Shahzad, Muhammad

    2016-03-01

    Oxidative stress and glycation processes have a combined effect on diabetes related complications. Crude plant extracts and plant derived compounds possessing both antiglycation and antioxidant activities have a high therapeutic potential for treating these complications. Antioxidant, antiglycation, anti-lipid per oxidation and cytotoxic activities of crude methanol extract and solvent fractions of Hypericum androsaemum L. (Hypericaceae) were evaluated and correlated with total content of phenolics and flavonoids. Significant radical scavenging activity was observed for the methanol extract against 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical used as a basis for antioxidant activity with IC50 value of 92.70±2.85 μg mL(-1) (96.20±2.34% inhibition at 500 μg mL(-1)). In case of anion scavenging activity the results were not very significant (33.20±1.22% inhibition at 500 μg mL(-1)). Anti-lipid per oxidation activity was highest for n-hexane fraction (67.83±1.33% inhibition at 500 μg mL(-1)) while the ethyl acetate fraction had the highest antiglycation activity (62.77±2.54% inhibition at 500 μg mL(-1)). Statistically significant correlation was determined for antioxidant and antiglycation activity and phenolic and flavonoid contents. In cytotoxicity assay all the extracts had IC50 values >30 μg mL(-1) as compared to the standard cycloheximide (IC50 value 0.084±0.1 μg mL(-1)). The polar extracts of H. androsaemum can be a good source of non-toxic compounds with antioxidant, anti-lipid per oxidation and antiglycation activities.

  9. Health Screening

    Science.gov (United States)

    Screenings are tests that look for diseases before you have symptoms. Screening tests can find diseases early, when they're easier to treat. You can get some screenings in your doctor's office. Others need special equipment, ...

  10. Screening of radical scavenging activity of some medicinal and aromatic plant extracts

    NARCIS (Netherlands)

    Miliauskas, G.; Venskutonis, R.P.; Beek, van T.A.

    2004-01-01

    Extracts of 12 medicinal and aromatic plants were investigated for their radical scavenging activity using DPPH and ABTS assays: Salvia sclarea, Salvia glutinosa, Salvia pratensis, Lavandula angustifolia, Calendula officinalis, Matricaria recutita, Echinacea purpurea, Rhaponticum carthamoides, Jugla

  11. Screening of antibacterial activity of raspberry (Rubus idaeus L. fruit and pomace extracts

    Directory of Open Access Journals (Sweden)

    Velićanski Aleksandra S.

    2012-01-01

    Full Text Available Antibacterial activity of fruit and pomace extracts (concentration 50 mg/ml of two raspberry (Rubus idaeus L. cultivars (Meeker and Willamette was tested against selected Gram-positive and Gram-negative bacteria (reference and wild strains. Disc diffusion method with 15 μl of extracts and agar-well diffusion method with 50 and 100 μl were used. Antibiotic (cefotaxime/clavulanic acid was used as a control. Both raspberry fruit extracts showed the strongest antibacterial activity against Pseudomonas aeruginosa (wild strain and Bacillus cereus, where the largest clear zones (without growth appeared. Escherichia coli was the most resistant strain, with only zone of reduced growth. The highest antibacterial activity of pomace extracts was against Staphylococcus aureus and Staphylococcus saprophyticus. There were no differences in the antibacterial activity between cultivars for both fruit and pomace extracts. [Projekat Ministarstva nauke Republike Srbije, br. TR 31044

  12. PHYTOCHEMICAL SCREENING AND ANTIBACTERIAL ACTIVITY FROM NERIUM OLEANDER AND EVALUVATE THEIR PLANT MEDIATED NANOPARTICLE SYNTHESIS

    Directory of Open Access Journals (Sweden)

    R.S. Suganya

    2012-05-01

    Full Text Available Phytochemical and antibacterial activity of essential oils obtained from Nerium oleander leaf with the help of three different extracts like ethanol, Methanol, and acetone. In this aqueous leaf extracts confirms the presence of various phytochemicals. To evaluate the antibacterial activities of these aqueous extracts were determined by disc diffusion method. From these three extracts methanol shows strong antibacterial effect on Klebsiella, Pseudomonas, Alkaligenes except Acinetobacter. None of the leaf extracts show no more activity in Acinetobacter. Biologically synthesized nanoparticles have been widely used in the field of medicine. Shade dried leaves of Nerium oleander was used for the synthesis of silver nanoparticles. UV- Visible spectroscopy studies were carried out to assess the formation of Ag nanoparticles. Scanning electron microscope (SEM was used to characterize the Ag nanoparticle. To compare the antimicrobial activity of silver nanoparticles with the different leaf extracts.

  13. In vitro screening of traditional medicines for anti-HIV activity: memorandum from a WHO meeting.

    OpenAIRE

    1989-01-01

    Many plant products are being used by patients with acquired immunodeficiency syndrome (AIDS) in some countries without any scientific proof that they possess anti-HIV (human immunodeficiency virus) activity. Traditional healers are now offering their remedies for scientific evaluation, and a few studies provide information on the inhibitory activity against HIV of plants such as Viola yedoensis, Arctium lappa, Epimedium grandiflorum, Glycyrrhiza uralensis and Castanospermum australe. Natural...

  14. Versatile synthesis of probes for high-throughput enzyme activity screening

    OpenAIRE

    de Rond, Tristan; Peralta-Yahya, Pamela; Cheng, Xiaoliang; Northen, Trent R.; Keasling, Jay D.

    2013-01-01

    Mass spectrometry based technologies are promising as generalizable high-throughput assays for enzymatic activity. In one such technology, a specialized enzyme substrate probe is presented to a biological mixture potentially exhibiting enzymatic activity, followed by an in situ enrichment step using fluorous interactions and nanostructure-initiator mass spectrometry. This technology, known as Nimzyme, shows great potential but is limited by the need to synthesize custom substrate analogs. We ...

  15. Screening Approach to the Activation of Soil and Contamination of Groundwater at Linear Proton Accelerator Sites

    CERN Document Server

    Otto, Thomas

    The activation of soil and the contamination of groundwater at proton accelerator sites with the radionuclides 3H and 22Na are estimated with a Monte-Carlo calculation and a conservative soil- and ground water model. The obtained radionuclide concentrations show that the underground environment of future accelerators must be adequately protected against a migration of activation products. This study is of particular importance for the proton driver accelerator in the planned EURISOL facility.

  16. Screening of radical scavenging activity and polyphenol content of Bulgarian plant species

    OpenAIRE

    Milena Nikolova

    2011-01-01

    Background: Discovery of new plant species with antioxidant properties is a priority of many research teams. Most of the species included in this study are unstudied for antioxidant properties, but they are taxonomically related to reference plants with well-documented antioxidant activity. Materials and Methods: Free radical scavenging activity of plant extracts was evaluated using a 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay. An aluminum chloride colorimetric method was used for flavonoid d...

  17. PHYTOCHEMICAL SCREENING AND IN VITRO ANTIOXIDANT ACTIVITY OF AQUEOUS AND HYDROALCOHOLIC EXTRACT OF BACOPA MONNIERI LINN.

    Directory of Open Access Journals (Sweden)

    Monic Shah et al

    2012-09-01

    Full Text Available The present study was undertaken to investigate in-vitro antioxidant activity of aqueous and hydroalcoholic extract of whole plant of Bacopa monnieri Linn. Family- Scrophularaceae. The total Phenolic content was determined using folin ciocalteau method while the total flavonoid content was determined using aluminium chloride method. In vitro antioxidant activity was evaluated using the Reducing power assay, Hydrogen peroxide scavenging assay, nitric oxide scavenging activity, superoxide scavenging activity and hydroxyl radical scavenging activity. The hydroalcoholic extract had more phenol concentration (116.1 mg/g of extract when compared to aqueous extract (58 mg/g of extract. The flavonoid content was more in hydroalcoholic extract (242.6 mg/g of extract when compared to that of aqueous extract (202.8 mg/g of extract. The reducing power and hydrogen peroxide scavenging of the extract was found to be concentration dependent. The nitric oxide scavenging activity, superoxide scavenging activity and Hydroxyl radical scavenging activity was also concentration dependent with IC50 value being 254.70 µg/ml , 934.06 µg/ml and 510.60 µg/ml respectively for Aqueous extract and 169.22 µg/ml, 495.83 µg/ml, 488 µg/ml respectively for hydroalcoholic extract. The order of the antioxidant potency of the whole plant extract is Hydroalcoholic >> aqueous. The results clearly indicate that aqueous and hydroalcoholic extract of Bacopa monnieri has anti oxidant property which may be due to the presence of phenols and flavonoids.

  18. Parenting style, the home environment, and screen time of 5-year-old children; the 'be active, eat right' study

    NARCIS (Netherlands)

    L. Veldhuis (Lydian); A. van Grieken (Amy); C.M. Renders (Carry); R.A. Hirasing (Remy); H. Raat (Hein)

    2014-01-01

    textabstractIntroduction: The global increase in childhood overweight and obesity has been ascribed partly to increases in children's screen time. Parents have a large influence on their children's screen time. Studies investigating parenting and early childhood screen time are limited. In this stud

  19. An in vitro screening with emerging contaminants reveals inhibition of carboxylesterase activity in aquatic organisms.

    Science.gov (United States)

    Solé, Montserrat; Sanchez-Hernandez, Juan C

    2015-12-01

    Pharmaceuticals and personal care products (PPCPs) form part of the new generation of pollutants present in many freshwater and marine ecosystems. Although environmental concentrations of these bioactive substances are low, they cause sublethal effects (e.g., enzyme inhibition) in non-target organisms. However, little is known on metabolism of PPCPs by non-mammal species. Herein, an in vitro enzyme trial was performed to explore sensitivity of carboxylesterase (CE) activity of aquatic organisms to fourteen PPCPs. The esterase activity was determined in the liver of Mediterranean freshwater fish (Barbus meridionalis and Squalius laietanus), coastal marine fish (Dicentrarchus labrax and Solea solea), middle-slope fish (Trachyrhynchus scabrus), deep-sea fish (Alepocephalus rostratus and Cataetix laticeps), and in the digestive gland of a decapod crustacean (Aristeus antennatus). Results showed that 100μM of the lipid regulators simvastatin and fenofibrate significantly inhibited (30-80% of controls) the CE activity of all target species. Among the personal care products, nonylphenol and triclosan were strong esterase inhibitors in most species (36-68% of controls). Comparison with literature data suggests that fish CE activity is as sensitive to inhibition by some PPCPs as that of mammals, although their basal activity levels are lower than in mammals. Pending further studies on the interaction between PPCPs and CE activity, we postulate that this enzyme may act as a molecular sink for certain PPCPs in a comparable way than that described for the organophosphorus pesticides. PMID:26562051

  20. Extraction of flavonoids from Tagetes patula: process optimization and screening for biological activity

    Directory of Open Access Journals (Sweden)

    Vanessa M. Munhoz

    2014-10-01

    Full Text Available The flowers of Tagetes patula L., Asteraceae, commonly known as French marigold, are used in folk medicine as an antiseptic, diuretic, blood purifier and insect repellent. This study was conducted to optimize the extraction process through the biomonitoring of flavonoids, using a statistical mixture simplex-centroid design, to evaluate the effect of the solvents water, ethanol and acetone, as well as mixtures of these solvents, assessed by the total flavonoid content. The extracts were tested for dry residue, radical scavenging activity, chromatographic profile, and larvicidal activity. The acetone extract had the highest total flavonoid content, 25.13 ± 1.02% (4.07%; and the best radical scavenging activity, with IC50 of 15.74 μg/ml ± 1.09 (6.92%, but with lower dry residue, 6.62 ± 1.33% (20.10%. The water extracts showed higher levels of dry residue, but lower total flavonoid content and radical scavenging activity than the acetone extract. The positive correlation between the total flavonoid content and radical scavenging activity of the extracts showed that flavonoids contribute significantly to the antioxidant capacity. The statistical mixture design allowed us to optimize the extraction of flavonoids from flowers of T. patula, with acetone as the best extraction solvent. Preliminary studies on the biological activity of the optimized extracts demonstrated a larvicidal effect of the acetone extract on Aedes aegypti mosquitoes.

  1. Phytochemical screening and evaluation of antioxidant activities of Dracocephalum kotschyi and determination of its luteolin content

    Science.gov (United States)

    Kamali, Mansureh; Khosroyar, Susan; Kamali, Hossein; Ahmadzadeh Sani, Tooba; Mohammadi, Ameneh

    2016-01-01

    Objective: Dracocephalum kotschyi (Lamiaceae family) has been used in traditional medicine for stomach and liver disorders, headache and congestion. In the present study, we have investigated phytochemical properties and antioxidant activities of dichloromethane, ethyl acetate and methanol extracts of D.kotschyi. Material and Methods: Antioxidant activities of extracts were evaluated using the integration of HPLC-DPPH and ferric reducing antioxidant power (FRAP) methods. In addition, the luteolincontent was determined using HPLC method. Results: The highest antioxidant activity was observed for the methanol extract (among the three tested extracts) showing 50% DPPH scavenging activity at 4.85µg/ml as compared to butylated hydroxy toluene (BHT) and ascorbic acid (3.00 µg/ml, 0.97 µg/ml). Also, luteolin was detected in methanol extract; it was identified by comparing its retention time and DAD spectra with standard and it was one of antioxidant components of this plant. In addition, the antioxidant activity of methanol extract was higher than BHT, in FRAP assay. Total phenolic content was in the range of 11.62-22.29 mg Gallic acid /gram of dry extract and flavonoid content was in the range of 3.97-5.042 mg Quercetin/ gram of extract for dichloromethane, ethyl acetate and methanol extracts. The quantity of luteolin in D.kotschyiwas found to be 1061.005 µg/g of dried plant. Conclusion: The results of this investigation indicated that luteolin plays major role in the antioxidant activity of the plant.

  2. Preliminary screening of Cuscuta reflexa stems for Anti inflammatory and cytotoxic activity

    Institute of Scientific and Technical Information of China (English)

    Pavan Bhausaheb Udavant; Suggala Venkata Satyanarayana; Chandrashekhar Devidas Upasani

    2012-01-01

    Objective: Evaluation of preliminary antiinflammatory and cytotoxic activities of a parasitic plant Cuscuta reflexa. Methods: Human red blood stabilizing activity was used for the evaluation of in vitro antiinflammatory activity and Brine shrimp lethality assay was used to assess the cytotoxic potential of extract of stems of Cuscuta reflexa. Results: Methanolic extract and Ethyl acetate fraction of methanolic extract of Cuscuta reflexa (MECR & EAMECR resp.) were found to have significant antiinflammatory and cytotoxic activity with inhibitory concentration IC50%values 277.83 μg/ml & 214.94 μg/ml in HRBC stabitlity assay[table 01], and lethal concentration LC50% 257.73 μg/ml 184.86 μg/ml in BSLA respectively[table 02]. Conclusions: Amongst various extracts evaluated for cytotoxicity and antiinflammatory activities, methanolic extract of Cuscutareflexa (MECR) and its ethyl acetate soluble fraction (EAMECR) show significant cytotoxic as well as antiinflammatory activities which may be due to the presence of phenols, polyphenols and flavonoids.

  3. An in vitro screening with emerging contaminants reveals inhibition of carboxylesterase activity in aquatic organisms.

    Science.gov (United States)

    Solé, Montserrat; Sanchez-Hernandez, Juan C

    2015-12-01

    Pharmaceuticals and personal care products (PPCPs) form part of the new generation of pollutants present in many freshwater and marine ecosystems. Although environmental concentrations of these bioactive substances are low, they cause sublethal effects (e.g., enzyme inhibition) in non-target organisms. However, little is known on metabolism of PPCPs by non-mammal species. Herein, an in vitro enzyme trial was performed to explore sensitivity of carboxylesterase (CE) activity of aquatic organisms to fourteen PPCPs. The esterase activity was determined in the liver of Mediterranean freshwater fish (Barbus meridionalis and Squalius laietanus), coastal marine fish (Dicentrarchus labrax and Solea solea), middle-slope fish (Trachyrhynchus scabrus), deep-sea fish (Alepocephalus rostratus and Cataetix laticeps), and in the digestive gland of a decapod crustacean (Aristeus antennatus). Results showed that 100μM of the lipid regulators simvastatin and fenofibrate significantly inhibited (30-80% of controls) the CE activity of all target species. Among the personal care products, nonylphenol and triclosan were strong esterase inhibitors in most species (36-68% of controls). Comparison with literature data suggests that fish CE activity is as sensitive to inhibition by some PPCPs as that of mammals, although their basal activity levels are lower than in mammals. Pending further studies on the interaction between PPCPs and CE activity, we postulate that this enzyme may act as a molecular sink for certain PPCPs in a comparable way than that described for the organophosphorus pesticides.

  4. Screening of immunomodulatory activity of total and protein extracts of some Moroccan medicinal plants.

    Science.gov (United States)

    Daoudi, Abdeljlil; Aarab, Lotfi; Abdel-Sattar, Essam

    2013-04-01

    Herbal and traditional medicines are being widely used in practice in many countries for their benefits of treating different ailments. A large number of plants in Morocco were used in folk medicine to treat immune-related disorders. The objective of this study is to evaluate the immunomodulatory activity of protein extracts (PEs) of 14 Moroccan medicinal plants. This activity was tested on the proliferation of immune cells. The prepared total and PEs of the plant samples were tested using MTT (3-(4,5-dimethylthiazol-2yl)-2,5-diphenyltetrazolium bromide) assay on the splenocytes with or without stimulation by concanavalin-A (Con-A), a mitogenic agent used as positive control. The results of this study indicated different activity spectra. Three groups of activities were observed. The first group represented by Citrullus colocynthis, Urtica dioica, Elettaria cardamomum, Capparis spinosa and Piper cubeba showed a significant immunosuppressive activity. The second group that showed a significant immunostimulatory activity was represented by Aristolochia longa, Datura stramonium, Marrubium vulgare, Sinapis nigra, Delphynium staphysagria, Lepidium sativum, Ammi visnaga and Tetraclinis articulata. The rest of the plant extracts did not alter the proliferation induced by Con-A. This result was more important for the PE than for the total extract. In conclusion, this study revealed an interesting immunomodulating action of certain PEs, which could explain their traditional use. The results of this study may also have implications in therapeutic treatment of infections, such as prophylactic and adjuvant with cancer chemotherapy. PMID:22301818

  5. Analysis of Anti-infection in One Case of Pulmonary Abscess%一例肺脓肿患者的抗感染方案分析

    Institute of Scientific and Technical Information of China (English)

    金旭辉; 裴素娟; 柳小飞

    2016-01-01

    Objective: To investigate the effect of clinical pharmacists in the clinical treatment of a case of pulmonary abscess by clinical pharmacists. Methods: Pharmacistsparticipatedand assisted doctors in a case of patients with lung abscesses, for theanti-infection treatment.Results: The clinical pharmacists involved in the treatment of patients with anti-infection treatment, and improved the effect of drug treatment.Conclusion: Clinical pharmacists directly participated in the formulation and adjustment of the treatment plan, andpromoted the clinical rational drug use.%目的:通过临床药师参与并分析对一例肺脓肿患者抗感染治疗,探讨临床药师在临床治疗中发挥的作用。方法:药师通过参与一例完整的肺脓肿病例的治疗,与临床医生一起制定抗感染治疗方案并协助医生及时调整。结果:该患者在临床医生与临床药师一起的抗感染治疗下,获得了很好的治疗效果,临床治愈出院。结论:临床药师直接参与医生治疗方案的制定与调整可促进临床合理用药。

  6. Development and Validation of a Novel Leishmania donovani Screening Cascade for High-Throughput Screening Using a Novel Axenic Assay with High Predictivity of Leishmanicidal Intracellular Activity

    OpenAIRE

    Andrea Nühs; Manu De Rycker; Sujatha Manthri; Eamon Comer; Scherer, Christina A.; Schreiber, Stuart L.; Jean-Robert Ioset; Gray, David W.

    2015-01-01

    Visceral leishmaniasis is an important parasitic disease of the developing world with a limited arsenal of drugs available for treatment. The existing drugs have significant deficiencies so there is an urgent need for new and improved drugs. In the human host, Leishmania are obligate intracellular parasites which poses particular challenges in terms of drug discovery. To achieve sufficient throughput and robustness, free-living parasites are often used in primary screening assays as a surroga...

  7. Screening of POP pollution by AChE and EROD activities in Zebra mussels from the Italian Great Lakes.

    Science.gov (United States)

    Binelli, A; Ricciardi, Francesco; Riva, Consuelo; Provini, Alfredo

    2005-12-01

    The increase of ethoxyresorufin dealkylation (EROD) and the inhibition of acetylcholinesterase (AChE) as biomarkers have been commonly used in vertebrates for the persistent organic pollutants (POPs) biomonitoring of aquatic environments, but very few studies have been performed for invertebrates. Previous researches demonstrated the interference due to some chemicals on EROD and AChE activities of the freshwater bivalve Zebra mussel (Dreissena polymorpha) in laboratory and field studies, showing its possible use for the screening of POP effects. We investigated the contamination of the Italian sub-alpine great lakes (Maggiore, Lugano, Como, Iseo, Garda) by the biomarker approach on Zebra mussel specimens collected at 17 sampling sites with different morphometric characteristics and anthropization levels. Results showed a homogeneous contamination of AChE inhibitors in Lake Garda, Maggiore, Como and Iseo with values ranging from 0.5 to 3 nmol/min/mg proteins and with an average inhibition of about 66% to controls. The planar compounds pollution, able to activate the EROD activity, seems higher in some sampling stations of Lake Garda, Como and Iseo (2-4 pmol/min/mg proteins) than that measured in Lake Lugano (1.5-3 pmol/min/mg proteins). On the contrary, the enzyme activity in Lake Maggiore showed an interesting opposite effect of AhR-binding compounds and trace metals. Finally, the possible use of Zebra mussel specimens maintained at laboratory conditions as controls against the selection of the less polluted sampling site is discussed.

  8. Screening of antioxidant activity and volatile compounds composition of Chamerion angustifolium (L.) Holub ecotypes grown in Lithuania.

    Science.gov (United States)

    Kaškonienė, Vilma; Maruška, Audrius; Akuņeca, Ieva; Stankevičius, Mantas; Ragažinskienė, Ona; Bartkuvienė, Violeta; Kornyšova, Olga; Briedis, Vitalis; Ugenskienė, Rasa

    2016-06-01

    Since biological activity of medicinal plants is dependent on cultivation area, climatic conditions, developmental stage, genetic modifications and other factors, it is important to study flora present in different growing sites and geographical zones. This study was focused on screening of antioxidant activity of C. angustifolium harvested in six different locations in Lithuania. The total contents of phenolic compounds, flavonoids and 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity were evaluated by spectrophotometric methods. A correlation between radical scavenging activity and total phenolic compounds content was observed (correlation coefficient 0.98). HPLC with online post-column DPPH radical scavenging reaction detection was used for the separation of extracts. Oenothein B, rutin and one unidentified compound were predominant. Volatile compounds were analysed using solid-phase microextraction coupled with gas chromatography-mass spectrometry. Based on the analysis of volatiles, all samples were classified into two chemotypes: (I) with predominant α- and β-caryophyllenes and (II) with predominant anethole. PMID:26222982

  9. Evaluation design of New York City's regulations on nutrition, physical activity, and screen time in early child care centers.

    Science.gov (United States)

    Breck, Andrew; Goodman, Ken; Dunn, Lillian; Stephens, Robert L; Dawkins, Nicola; Dixon, Beth; Jernigan, Jan; Kakietek, Jakub; Lesesne, Catherine; Lessard, Laura; Nonas, Cathy; O'Dell, Sarah Abood; Osuji, Thearis A; Bronson, Bernice; Xu, Ye; Kettel Khan, Laura

    2014-01-01

    This article describes the multi-method cross-sectional design used to evaluate New York City Department of Health and Mental Hygiene's regulations of nutrition, physical activity, and screen time for children aged 3 years or older in licensed group child care centers. The Center Evaluation Component collected data from a stratified random sample of 176 licensed group child care centers in New York City. Compliance with the regulations was measured through a review of center records, a facility inventory, and interviews of center directors, lead teachers, and food service staff. The Classroom Evaluation Component included an observational and biometric study of a sample of approximately 1,400 children aged 3 or 4 years attending 110 child care centers and was designed to complement the center component at the classroom and child level. The study methodology detailed in this paper may aid researchers in designing policy evaluation studies that can inform other jurisdictions considering similar policies. PMID:25321635

  10. Screening of some medicinal plants from cameroon for beta-lactamase inhibitory activity.

    Science.gov (United States)

    Gangoué-Piéboji, Joseph; Baurin, Stéphane; Frère, Jean-Marie; Ngassam, Pierre; Ngameni, Bathelemy; Azebaze, Anatole; Pegnyemb, Dieudonné Emmanuel; Watchueng, Jean; Goffin, Colette; Galleni, Moreno

    2007-03-01

    In efforts to find new bioactive beta-lactamase inhibitors, this study investigated 16 Cameroonian plants belonging to 10 families which were evaluated for anti-beta-lactamase activity. The investigation showed that extracts 2, 6, 3 and 5 of the 16 plants investigated presented interesting in vitro beta-lactamase inhibition (over 90%), respectively, of the beta-lactamases TEM-1, OXA-10, IMP-1 and P99. These extracts were from Mammea africana (all beta-lactamases), Garcinia lucida, G. kola (OXA-10, IMP-1 and P99), Bridelia micrantha (OXA-10, P99), Ochna afzelii (OXA-10, P99), Prunus africana (IMP-1) and Adenia lobata (TEM-1). After elimination of tannins (according to the European Pharmacopoeia) the extracts from B. micrantha, G. lucida and M. africana were tested further for their anti-beta-lactamase activity. The extracts from B. micrantha and G. lucida exhibited potent inhibitory activity, respectively, of beta-lactamase OXA-10 (IC(50) = 0.02 mg/mL) and P99 (IC(50) = 0.01 mg/mL). The anti-beta-lactamase activity of M. africana extract was weak. The isolation and the structural elucidation of the active constituents of G. lucida and B. micrantha will provide useful leads in the development of beta-lactamase inhibitors.

  11. Daily Physical Activity and Screen Time, but Not Other Sedentary Activities, Are Associated with Measures of Obesity during Childhood

    OpenAIRE

    Shoo Thien Lee; Jyh Eiin Wong; Safii Nik Shanita; Mohd Noor Ismail; Paul Deurenberg; Bee Koon Poh

    2014-01-01

    Childhood obesity is related to low physical activity level and a sedentary lifestyle. The aim of this study was to assess the physical activity level and sedentary behaviour of Malaysian children aged 7 to 12 years and to examine their association with body mass index (BMI), BMI-for-age Z-score (BAZ), body fatness (%BF) and waist circumference (WC). A total of 1736 children, representing all ethnic groups were recruited from six regions of Malaysia. Anthropometric measurements included body ...

  12. A target-based high throughput screen yields Trypanosoma brucei hexokinase small molecule inhibitors with antiparasitic activity.

    Directory of Open Access Journals (Sweden)

    Elizabeth R Sharlow

    Full Text Available BACKGROUND: The parasitic protozoan Trypanosoma brucei utilizes glycolysis exclusively for ATP production during infection of the mammalian host. The first step in this metabolic pathway is mediated by hexokinase (TbHK, an enzyme essential to the parasite that transfers the gamma-phospho of ATP to a hexose. Here we describe the identification and confirmation of novel small molecule inhibitors of bacterially expressed TbHK1, one of two TbHKs expressed by T. brucei, using a high throughput screening assay. METHODOLOGY/PRINCIPAL FINDINGS: Exploiting optimized high throughput screening assay procedures, we interrogated 220,233 unique compounds and identified 239 active compounds from which ten small molecules were further characterized. Computation chemical cluster analyses indicated that six compounds were structurally related while the remaining four compounds were classified as unrelated or singletons. All ten compounds were approximately 20-17,000-fold more potent than lonidamine, a previously identified TbHK1 inhibitor. Seven compounds inhibited T. brucei blood stage form parasite growth (0.03activity. None of the compounds displayed structural similarity to known hexokinase inhibitors or human African trypanosomiasis therapeutics. CONCLUSIONS/SIGNIFICANCE: The novel chemotypes identified here could represent leads for future therapeutic development against the African trypanosome.

  13. Development and Implementation of a Smartphone Application to Promote Physical Activity and Reduce Screen-time in Adolescent Boys

    Directory of Open Access Journals (Sweden)

    David Revalds Lubans

    2014-05-01

    Full Text Available Purpose: The primary aim is to describe the development and implementation of a smartphone application (app designed to promote physical activity and reduce screen-time in adolescent boys ‘at risk’ of obesity from low-income communities.Methods: An app was developed to support the delivery of a face-to-face school-based obesity prevention program known as the ‘Active Teen Leaders Avoiding Screen-time’ (ATLAS program. ATLAS was guided by self-determination theory and social cognitive theory and evaluated using a cluster randomized controlled trial with 361 boys (12.7± 0.5 years in 14 secondary schools. Following the completion of the study, participants in the intervention group completed a process evaluation questionnaire and focus groups were conducted with 42 students to explore their general perceptions of the ATLAS program and their experience with the smartphone app. Barriers and challenges encountered in the development, implementation and evaluation of the app are also described.Results: Participation in the study was not contingent on ownership of a smartphone, but 70% of participants in the intervention group reported having access to a smartphone or tablet device. Focus group participants reported an enjoyment of the program, and felt that it had provided them with new skills, techniques, and routines for the future. However, their engagement with the smartphone app was limited, due to a variety of reasons. Barriers to the implementation and evaluation of the app included limited access to smartphone devices, technical problems with the push notifications, lack of access to usage data and the challenges of maintaining participants’ interest in using the app.Conclusions: Although participants reported high levels of satisfaction with the ATLAS program in general, the smartphone app was not used extensively. Additional strategies and features may be needed to enhance engagement in adolescent boys.

  14. Screening of Probiotic Activities of Lactobacilli Strains Isolated from Traditional Tibetan Qula, A Raw Yak Milk Cheese.

    Science.gov (United States)

    Zhang, Bei; Wang, Yanping; Tan, Zhongfang; Li, Zongwei; Jiao, Zhen; Huang, Qunce

    2016-10-01

    In this study, 69 lactobacilli isolated from Tibetan Qula, a raw yak milk cheese, were screened for their potential use as probiotics. The isolates were tested in terms of: Their ability to survive at pH 2.0, pH 3.0, and in the presence of 0.3% bile salts; tolerance of simulated gastric and intestinal juices; antimicrobial activity; sensitivity against 11 specific antibiotics; and their cell surface hydrophobicity. The results show that out of the 69 strains, 29 strains (42%) had survival rates above 90% after 2 h of incubation at pH values of 2.0 or 3.0. Of these 29 strains, 21 strains showed a tolerance for 0.3% bile salt. Incubation of these 21 isolates in simulated gastrointestinal fluid for 3 h revealed survival rates above 90%; the survival rate for 20 of these isolates remained above 90% after 4 h of incubation in simulated intestinal fluid. The viable counts of bacteria after incubation in simulated gastric fluid for 3 h and simulated intestinal fluid for 4 h were both significantly different compared with the counts at 0 h (pcasei 1,133 (92%), Lactobacillus plantarum 1086-1 (82%), Lactobacillus casei 1089 (81%), Lactobacillus casei 1138 (79%), Lactobacillus buchneri 1059 (78%), Lactobacillus plantarum1141 (75%), and Lactobacillus plantarum 1197 (71%). Together, these results suggest that these seven strains are good probiotic candidates, and that tolerance against bile acid, simulated gastric and intestinal juices, antimicrobial activity, antibiotic resistance, and cell surface hydrophobicity could be adopted for preliminary screening of potentially probiotic lactobacilli. PMID:26954218

  15. Cytokine, Chemokine and Immune Activation Pathway Profiles in Celiac Disease: An Immune System Activity Screening by Expression Macroarrays

    Directory of Open Access Journals (Sweden)

    José A. Garrote

    2008-01-01

    Full Text Available The aims of the study were to assess the usefulness of expression macroarrays to determine the pattern of expression of cytokines, chemokines and molecules related to immune system activation pathways, in non-stimulated intact intestinal tissue specimens from patients with active CD (aCD and on a gluten-free diet (GFD, to compare it with two groups of controls with either normal or altered mucosal architecture, and to establish putative targets for diagnostic markers or therapeutic intervention. We have experienced the lack of sensitivity to detect signal of genes with low level of expression. In spite of that, active CD seems to show a Th1 cytokine pattern, but with signs of Th2 activity. Cytokines such as IL-9, IL-11, IL-21 or MIF might be involved in mucosal inflammation in CD. In GFD, some memory cells and DC’s activity remains, and factors that maintain this remnant activation might be responsible of the fast mucosal response on gluten challenge. STAT3 and STAT5 pathways, and their regulatory molecules SOCS’s may result keys for understanding mucosal inflammation in gut and putative targets for further research.

  16. Screening of Malian medicinal plants for antifungal, larvicidal, molluscicidal, antioxidant and radical scavenging activities.

    Science.gov (United States)

    Diallo, D; Marston, A; Terreaux, C; Touré, Y; Paulsen, B S; Hostettmann, K

    2001-08-01

    A total of 78 different extracts from 20 medicinal plants belonging to 14 plant families from Mali were tested for their antifungal, larvicidal, molluscicidal, antioxidant and radical scavenging activities. Dichloromethane, methanol, water and ethanol extracts were used. TLC autobiography for antifungal activity was run with Cladosporium cucumerinum and Candida albicans. Extracts were also tested on the larvae of the mosquitoes Aedes aegypti, Anopheles gambiae and Culex quinquefasciatus. Molluscicidal activities were established with the snails Biomphalaria glabrata, Biomphalaria pfeifferi and Bulinus truncatus. beta-Carotene and DPPH solutions sprayed on TLC plates were used for antioxidant and radical scavenging assays. Of the extracts investigated, 20% were antioxidant and radical scavengers, 19% fungicidal, 30% were larvicidal and 11% were molluscicidal. Three of the plant extracts, from Cussonia barteri (Araliaceae), Glinus oppositifolius (Aïzoaceae) and Lannea velutina (Anacardiaceae) gave positive responses in all four tests. PMID:11507731

  17. Data on synthesis of methylene bisphosphonates and screening of their inhibitory activity towards HIV reverse transcriptase.

    Science.gov (United States)

    Yanvarev, D V; Korovina, A N; Usanov, N N; Khomich, O A; Vepsäläinen, J; Puljula, E; Kukhanova, M K; Kochetkov, S N

    2016-09-01

    Inorganic pyrophosphate (PPi) mimetics designed on a basis of methylenediphosphonic acid backbone are promising inhibitors of two key HIV replication enzymes, IN [1] and RT [2]. Herein, we present chemical synthesis of eleven methylenebisphosphonates (BPs) with their NMR and HRMS analysis synthesized via five different ways. Also, we present data on inhibition of HIV RT catalyzed phosphorolysis and polymerization by synthesized BPs using two methods based on denaturing urea PAGE. Tests were also performed for thymidine analogue mutations reverse transcriptase (TAM RT), which was expressed and purified for that. Structure-activity relationships and inhibitory activity data of synthesized BPs are presented in "Methylene bisphosphonates as the inhibitors of HIV RT phosphorolytic activity" [2]. PMID:27547792

  18. PRELIMINARY PHYTOCHEMICAL SCREENING OF ANTIBACTERIAL ACTIVITY OF PALMYRA PALM ( BORASSUS FLABELLIFER ROOT EXTRACT

    Directory of Open Access Journals (Sweden)

    Saravanan C., Priya B.*, Asir Bradley S. and Uma Sundaram

    2012-11-01

    Full Text Available The phytochemical constituents of Borassus flabellifer was identified and evaluated the antibacterial activity of the acetone, benzene, chloroform, ethanol and methanol extracts. A phytoconstituent analysis of alkaloids, glycosides, terpenoids, steroids, flavonoids, tannins, phenols and saponins were performed on the various solvent extracts. Antibacterial activity was analyzed by agar well diffusion method against five pathogenic microorganisms, E. coli, S. aureus, K. pneumonia, P. aeruginosa and B. subtilis. The maximum zone of inhibition was exhibited for E.coli (14mm; P. aeruginosa (13mm and B. subtilis (11mmagainst compared to tested micro organisms. The methanolic extract of the palm root has showed consistently significant inhibitory activity on different bacterial species tested. Furthermore, identification of bioactive compounds will be analyzed.

  19. Screening of the topical anti-inflammatory activity of some Central American plants.

    Science.gov (United States)

    Sosa, S; Balick, M J; Arvigo, R; Esposito, R G; Pizza, C; Altinier, G; Tubaro, Aurelia

    2002-07-01

    Hexane, chloroform and methanol extracts of seven herbal drugs used in the folk medicine of Central America against skin disorders (Aristolochia trilobata leaves and bark, Bursera simaruba bark, Hamelia patens leaves, Piper amalago leaves, and Syngonium podophyllum leaves and bark) were evaluated for their topical anti-inflammatory activity against the Croton oil-induced ear oedema in mice. Most of the extracts induced a dose-dependent oedema reduction. The chloroform extract of almost all the drugs exhibited interesting activities with ID(50) values ranging between 108 and 498 micro g/cm(2), comparable to that of indomethacin (93 micro g/cm(2)). Therefore, the tested plants are promising sources of principles with high anti-inflammatory activity.

  20. Screening of anti-bacterial activity of medicinal plants from Belize (Central America).

    Science.gov (United States)

    Camporese, A; Balick, M J; Arvigo, R; Esposito, R G; Morsellino, N; De Simone, F; Tubaro, A

    2003-07-01

    Twenty-one extracts from seven herbal drugs, Aristolochia trilobata (Aristolochiaceae) leaves and bark, Bursera simaruba (Burseraceae) bark, Guazuma ulmifolia (Sterculiaceae) bark, Hamelia patens (Rubiaceae) leaves and Syngonium podophyllum (Araceae) leaves and bark, used in traditional medicine of Belize (Central America) as deep and superficial wound healers, were evaluated for their anti-bacterial properties. Activity was tested against standard strains of Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853, Staphylococcus aureus ATCC 25923 and Enterococcus faecalis ATCC 29212. Almost all the extracts were able to inhibit the growth of one or more of the bacterial strains, except that of Enterococcus faecalis. For the first time an anti-microbial activity is reported for Aristolochia trilobata as well as for Syngonium podophyllum. The hexane extracts of Aristolochia trilobata leaves and bark were the most active extracts against Staphylococcus aureus (MIC=0.31 and 0.625mg/ml, respectively).

  1. Phytochemical screening and evaluation of antioxidant activities of Dracocephalum kotschyi and determination of its luteolin content

    Directory of Open Access Journals (Sweden)

    Mansureh Kamali

    2016-06-01

    Full Text Available Objective: Dracocephalum kotschyi (Lamiaceae family has been usedin traditional medicine for stomach and liver disorders, headache and congestion. In the present study, we have investigated phytochemical properties and antioxidant activities of dichloromethane, ethyl acetate and methanol extracts of D.kotschyi. Material and Methods: Antioxidant activities of extracts were evaluated using the integration of HPLC-DPPH and ferric reducing antioxidant power (FRAP methods. In addition, the luteolincontent was determined using HPLC method. Results: The highest antioxidant activity was observed for the methanol extract (among the three tested extracts showing 50% DPPH scavenging activity at 4.85µg/ml as compared to butylated hydroxy toluene (BHT and ascorbic acid (3.00 µg/ml, 0.97 µg/ml. Also, luteolin was detected in methanol extract; it was identified by comparing its retention time and DAD spectra with standard and it was one of antioxidant components of this plant. In addition, the antioxidant activity of methanol extract was higher than BHT, in FRAP assay. Total phenolic content was in the range of 11.62-22.29 mg Gallic acid /gram of dry extract and flavonoid content was in the range of 3.97-5.042 mg             Quercetin/ gram of extract for dichloromethane, ethyl acetate and methanol extracts. The quantity of luteolin in D.kotschyiwas found to be 1061.005 µg/g of dried plant. Conclusion: The results of this investigation indicated that luteolin plays major role in the antioxidant activity of the plant.

  2. Phytochemical screening and antimicrobial activities of the constituents isolated from Koelreuteria paniculata leaves.

    Science.gov (United States)

    Ghahari, Somayeh; Alinezhad, Heshmatollah; Nematzadeh, Ghorban Ali; Ghahari, Sajjad

    2015-01-01

    Methanolic extract of Golden rain leaves was fractionated by column chromatography on silica gel and 18 fractions were obtained. Antimicrobial activities of fractions were investigated against Bacillus subtilis, Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa as quality control bacteria and fungus Pyricularia grisea which causes Blast disease in rice. Fractions showed more antibacterial activity at 0.04 g/mL concentration only on B. subtilis and S. aureus as gram positive bacteria. Also, three fractions indicated excellent antifungal effect on fungus P. grisea. Moreover, in the present study, fractions that showed very good effect on microorganisms were used for gas chromatography-mass spectrometry analysis to identify different phytochemicals. PMID:25813082

  3. Screening of Fungi from Chinese Medical Plants for Anti-Human Immunodeficiency Virus Type 1 Activity

    Institute of Scientific and Technical Information of China (English)

    2006-01-01

    In order to isolate anti-human immunodeficiency virus (HIV) agents from natural products, 97 ethanolic extracts of 90 fungi were tested for their inhibitory activity on HIV-1. Most of the extracts tested were relatively non-toxic to human lymphocytic MT-4 cells, but extracts of some fungi exhibited potent anti-HIV activity in an in vitro 3-(4,5-dimethyl-2 thiazoyl)-2,5-diphenyl-2H-tetrazolium bromide assay with a selectivity index greater than 3. Most fungi were isolated from Dendrobium sp. and Taxus sp.

  4. Screening of Antibacterial Activities of Essential Oils from Selected Medicinal Plants

    International Nuclear Information System (INIS)

    Essential oils were extracted from the five medicinal plants (Syzygium aromaticum Linn, Cinnamoum tamala. Nees, Piper betle. Linn, Ocimum sanctum, Clausena exacavata Burn) by steam distillation method and percolation method with petroleum ether. These plants do not contain cyanogenic glycosides according to phytochemical tests. Essential oils from these plants were also tested on antimicrobial activity by agar well diffusion method. It was observed that essential oils extracted from these five plants have various effects on Gram-positive and Gram-negative bacteria and fungus. Among them, essential oils of Syzygium aromaticum possess the highest antimicrobial activity aganist all test organisms. B. pumalis and Calbican are the most susceptible to the five plants.

  5. Screening of selected pesticides for inhibition of CYP19 aromatase activity in vitro

    DEFF Research Database (Denmark)

    Vinggaard, A.M.; Hnida, C.; Breinholt, V.;

    2000-01-01

    range of hormone-mimicking effects. Twenty-two pesticides were tested for their ability to affect CYP19 aromatase activity in human placental microsomes using the classical [H-3](2)O method. Prochloraz, imazalil, propioconazole, fenarimol, triadimenol, triadimefon tall fungicides), and dicofol tan...... acaricide) gave rise to a statistically significant inhibition of aromatase activity. The IC(50)s of prochloraz, imazalil, propioconazole fenarimol, triadimenol, and triadimefon were calculated from dose-response curves to be 0.04, 0.34, 6.5, 10, 21 and 32 mu M, respectively, The IC50 Of dicofol was greater...

  6. Screening test for anti-Helicobacter pylori activity of traditional Chinese herbal medicines

    Institute of Scientific and Technical Information of China (English)

    2010-01-01

    AIM:To evaluate the anti-Helicobacter pylori (H.pylori) activity of 50 traditional Chinese herbal medicines in order to provide the primary evidence for their use in clinical practice.METHODS:A susceptibility test of water extract from 50 selected traditional Chinese herbal medicines for in vitro H.pylori Sydney strain 1 was performed with broth dilution method.Anti-H.pylori activity of the selected Chinese herbal medicines was evaluated according to their minimum inhibitory concentration (MIC).RESULTS:The ...

  7. 2009~2010年我院抗感染药物使用分析%Application analysis of anti-infective drugs in our hospital from 2009 to 2010

    Institute of Scientific and Technical Information of China (English)

    王诗鸿; 王秀中; 郑丽莹

    2012-01-01

    目的 了解我院抗感染药物的应用情况,为临床合理用药提供参考.方法 依托我院药品管理系统的原始数据,对我院2009~2010年抗感染药物的销售金额和用药频度(DDDs)等进行回顾性分析.结果 2009~2010年我院抗感染药物销售金额占药品销售总金额的比例呈下降趋势,在销售金额构成上,注射用药占90%以上,头孢菌素类、喹诺酮类位居前列,注射用头孢地嗪的销售金额和DDDs排序两年均居首位.结论我院抗感染药物使用基本合理,但仍存在少数品种过量使用,选择起点过高等问题,应进一步加强监管力度,促进抗感染药物的合理使用.%Objective To investigate and analyze the application of anti-infective drugs in our hospital, in order to provide references for rational clinical medication. Methods Depending on the original data from the management system of the drug stock, the data of anti-infective drugs application in our hospital from 2009 to 2010 were analyzed in respect of consumption sum, DDDs and so on. Results The consumption sum of anti-infective drugs in our hospital from 2009 to 2010 showed a downward trend. In the constitution of sales amount, intravenous drugs occupied more than 90% among all the anti-infective drugs. Cephalosporins and quinolones ranked the top places in respect of the consumption sum. Cefodizime for injection ranked the first place in respect of the consumption sum and DDDs from 2009 to 2010. Conclusion The use of antiinfective drugs is basically rational in our hospital. However, there are also some inappropriate problems such as drug overdose, selection of senior antibiotics and so on. It's necessary to strengthen supervision dynamicsc for promoting ration use of anti-infective drugs.

  8. Prevalence of Sexual Concerns and Sexual Dysfunction among Sexually Active and Inactive Men and Women with Screen-Detected Type 2 Diabetes

    DEFF Research Database (Denmark)

    Bjerggaard, Mette; Charles, Morten; Kristensen, Ellids;

    2015-01-01

    inactive men and women with type 2 diabetes and of sexual dysfunction (SD) among sexually active. METHODS: Data from the Anglo-Danish-Dutch Study of Intensive Treatment in People with Screen-Detected Diabetes in Primary Care-Denmark study was used. A total of 1,170 Danish patients with screen-detected type...... 2 diabetes attended a health examination, including assessment of sexual concerns using self-report questionnaires and of SD using the Female Sexual Function Index (FSFI-R) and the International Index of Erectile Function (IIEF-5) instruments. MAIN OUTCOME MEASURES: The main outcome measures used...... active and sexually inactive people with type 2 diabetes. Bjerggaard M, Charles M, Kristensen E, Lauritzen T, Sandbæk A, and Giraldi A. Prevalence of sexual concerns and sexual dysfunction among sexually active and inactive men and women with screen-detected type 2 diabetes. Sex Med 2015;3:302-310....

  9. The non-advertising effects of screen-based sedentary activities on acute eating behaviours in children, adolescents, and young adults. A systematic review.

    Science.gov (United States)

    Marsh, Samantha; Ni Mhurchu, Cliona; Maddison, Ralph

    2013-12-01

    Sedentary screen time may be an important determinant of childhood obesity. A number of potential mechanisms to explain the link between screen time and increased bodyweight have been proposed; however, the relationship appears to be best explained by the effects on dietary intake, which is attributed to either food advertising or effects independent of food advertising. Technological advances have allowed for greater accessibility and exposure to advertisement-free screen-based media. This review was conducted to systematically synthesise the evidence from laboratory based studies which have investigated the non-advertising effects of screen time (TV viewing, sedentary video games, and computer use) on dietary intake in children, adolescents, and young adults. MEDLINE, PubMed, PsychInfo, CINAHL, and Embase were searched from inception through 5 July 2013. Ten trials met the inclusion criteria and were included in the review. Risk of study bias was judged to range from low to high. Screen time in the absence of food advertising was consistently found to be associated with increased dietary intake compared with non-screen behaviours. Suggested explanations for this relationship included: distraction, interruption of physiologic food regulation, screen time as a conditioned cue to eat, disruption of memory formation, and the effects of the stress-induced reward system. Due to the limited number of high-quality studies available for this review, our findings are preliminary. More work is required to better establish the link between dietary intake and advertisement-free screen time and assess whether differences exist between the different screen-based activities. PMID:24001394

  10. Screening of Ficus religiosa leaves fractions for analgesic and anti-inflammatory activities

    Directory of Open Access Journals (Sweden)

    Vishal Gulecha

    2011-01-01

    Full Text Available Objective : To evaluate the different fractions of dried leaves of Ficus religiosa Linn for analgesic and anti-inflammatory activity using different models of pain and inflammation Materials and Methods : The analgesic activity of F. religiosa carried out using acetic acid-induced writhing in mice and tail flick test in rats. The anti-inflammatory activity was evaluated using carrageenan-induced rat paw edema and cotton pellet-granuloma formation in rats. Five different fractions (FRI, FRII, FRIII, FRIV and FRV of F. religiosa at the dose level of 20 and 40 mg/kg, p.o were tested. Results : The fraction FRI (40 mg/kg, p.o. and FRIII (40 mg/kg, p.o were found to be more effective (P<0.01 in preventing carrageenan induced rat paw edema, cotton pellet granuloma formation, and acetic acid induced writhing compared to the other fractions. FRI (20 mg/kg, p.o. and FRIII (20 mg/kg, p.o. were also found to be more effective in increasing latency period in tail flick method. Conclusion : Out of five different fractions of F. religiosa leaves tested, FRI and FRIII possess potent analgesic and anti-inflammatory activities against different models of inflammation and pain.

  11. Glycoside Hydrolases from a targeted Compost Metagenome, activity-screening and functional characterization

    Directory of Open Access Journals (Sweden)

    Dougherty Michael J

    2012-07-01

    Full Text Available Abstract Background Metagenomics approaches provide access to environmental genetic diversity for biotechnology applications, enabling the discovery of new enzymes and pathways for numerous catalytic processes. Discovery of new glycoside hydrolases with improved biocatalytic properties for the efficient conversion of lignocellulosic material to biofuels is a critical challenge in the development of economically viable routes from biomass to fuels and chemicals. Results Twenty-two putative ORFs (open reading frames were identified from a switchgrass-adapted compost community based on sequence homology to related gene families. These ORFs were expressed in E. coli and assayed for predicted activities. Seven of the ORFs were demonstrated to encode active enzymes, encompassing five classes of hemicellulases. Four enzymes were over expressed in vivo, purified to homogeneity and subjected to detailed biochemical characterization. Their pH optima ranged between 5.5 - 7.5 and they exhibit moderate thermostability up to ~60-70°C. Conclusions Seven active enzymes were identified from this set of ORFs comprising five different hemicellulose activities. These enzymes have been shown to have useful properties, such as moderate thermal stability and broad pH optima, and may serve as the starting points for future protein engineering towards the goal of developing efficient enzyme cocktails for biomass degradation under diverse process conditions.

  12. In vivo screening of essential oils of Skimmia laureola leaves for antinociceptive and antipyretic activity

    Directory of Open Access Journals (Sweden)

    Naveed Muhammad

    2013-03-01

    Conclusions: In vivo studies of SLO showed prominent antinociceptive and antipyretic activities with ample safety profile and thus provided pharmacological base for the traditional uses of the plant in various painful conditions and pyrexia. Additional detail studies are required to ascertain its clinical application.

  13. PHYTOCHEMICAL SCREENING AND ANTIOXIDANT ACTIVITY OF RHIZOME PART OF CURCUMA ZEDOARIA

    OpenAIRE

    Himaja M; Anand Ranjitha; Ramana M V; Anand M; Karigar Asif

    2010-01-01

    Curcuma zedoaria belongs to the family Zingiberaceae. The rhizome parts of Curcuma zedoaria was dried, extracted with different solvent by soxhlet extraction method. Phytochemical studies of all the crude extracts showed the presence of terpeniods, alkaloids, saponins, flavanoids, glycosides & carbohydrates, phenolic, tannins and phytosterols etc., The phytochemical results confirm that all extracts contains more important chemical constituents for various biological activities. Antioxidant a...

  14. Screening of BADH Activity of Borreria articularies (Linn. for the Inhibition of P. aeruginosa

    Directory of Open Access Journals (Sweden)

    Md Shamsuddin Sultan Khan

    2014-08-01

    Full Text Available Purposes: The present study was designed to investigate the antibacterial activities of the Ethanol and methanol extracts of the leaves of the plant Borreria articularies (Linn. effects on microbial growth inhibition in vitro, microbial cells in vivo and molecular enzyme (BADH targets in vitro.Methods: The preliminary phytochemicals of the extracts was determined by the standard methods and aliquoted with Thin Layer Chromatography (TLC and stored at 2-4oC. fluorescein diacetate (FDA and ethidium bromide (EB live-dead cell viability test for distinguishing the membrane active phytochemicals of the plant extract.  Betaine aldehyde dehydrogenase (BADH activity was assessed by spectrophotometer. Alkaloids, glycosides, steroids, gums, saponin and reducing sugar were found in extracts.Results: The results of the disc diffusion indicated that the crude extracts were able to inhibit the growth of bacteria within a concentration range of 0.5 to 2.0 mg/mL. At a similar concentration range (0.5 to 2.0 mg/mL the extract inhibited the growth of 90.12% of the tested microorganisms. Bacterial cell viability was found minor in the phytochemicals of crude extract. Also, constituents of crude extract inhibited the BADH activity to protect the adaptation in stress environment of the bacteria.Conclusion: Results of the present study showed the possible use of the studied plants extracts in the control of bacterial infections.   

  15. Screening a Mediterranean Sponge Axinella verrucosa For Antibacterial Activity in Comparison to Some Antibiotics

    Directory of Open Access Journals (Sweden)

    Alma Shabbar

    2013-03-01

    Full Text Available The antibacterial effect of crude extract of marine sponge Axinella verrucosa at room temperature against seven nosocomial bacteria and one fungal isolates including, Staphylococcus aureus, Pseudomonas aeruginosa, Acinetobacter septicus and Proteus vulgaris, Acinetobacter meningitis, Klebsiella pneumonia, E. coli and the fungal pathogen Candida albicans were studied by Kirby-Bauer disc diffusion assay and, the findings of antibacterial activity of crude methanolic extract sponge A. verrucosa were compared to the efficiency of some marketed antibiotics that were tested against the same bacteria at given concentrations. In result, it was found that MeOH crude extract of Axinella verrucosa is effective against Staphylococcus aureus, Pseudomonas aeruginosa, Acinetobacter septicus and Proteus vulgaris and except for its ineffectiveness against Acinetobacter meningitis, Klebsiella pneumonia, E. coli and the fungal pathogen Candida albicans. It was more active than Azithromycin and Gentamicin Against Proteus vulgaris and more efficient than ciprofloxacin against Acinetobacter septicus. Hexane and Ethyl acetate crude extracts derived from A. verrucosa revealed no activity against all bacterial and fungal pathogen. Sponge Axinella verrucosa remains an interesting source of new antibacterial metabolites with better activity than some antibiotics.

  16. Antioxidant activity screening of extracts from Sideritis species (Labiatae) grown in Bulgaria

    NARCIS (Netherlands)

    Koleva, I.; Linssen, J.P.H.; Beek, van T.A.; Evstatieva, L.N.; Kortenska, V.; Handjieva, N.

    2003-01-01

    Plant samples from several species and populations of the genus Sideritis (Labiatae) grown in Bulgaria (S scardica, S syriaca and S montana) were extracted with different solvents. Their antioxidant activities were determined by the -carotene bleaching test (BCBT), 2,2-diphenyl-1-picrylhydrazyl (DPP

  17. Preliminary screening of 44 plant extracts for anti-tyrosinase and antioxidant activities.

    Science.gov (United States)

    Ya, Wang; Chun-Meng, Zhao; Tao, Guo; Yi-Lin, Zhu; Ping, Zhao

    2015-09-01

    In order to find new tyrosinase inhibitors and antioxidant materials, we investigated 44 plants, which were evaluated for the anti-tyrosinase and antioxidant activities. The mushroom tyrosinase inhibition assay and 2, 2-Diphenyl-1- picrylhydrazyl (DPPH) radical scavenging assay were conducted to evaluate these activities. Among all tested plant extracts, Morus alba L. (positive control), Rhodiola crenulata (Hook. f. et Thoms.) H. Ohba, Momordica charantia L., Cuminum cyminum L. et al. exhibit higher tyrosinase inhibition. Rhodiola crenulata (Hook. f. et Thoms.) H. Ohba, Rosa rugosa Thunb. and Eugenia caryophyllata Thunb. perform the highest antioxidant activity, similar to vitamin C (the positive control). A low positive correlation is found in the DPPH radical scavenging and tyrosinase inhibition assay. Considering these factors, the extracts of Rhodiola crenulata (Hook. f. et Thoms.) H. Ohba, Alpinia officinarum Hance and Zanthoxylum bungeanum Maxim. exhibit high anti-tyrosinase and antioxidant activities and could be used in the cosmetic industry. Further studies are warranted to characterize the compounds responsible for the anti-tyrosinase and antioxidant properties of these plant extracts. PMID:26408894

  18. Screening for Antimicrobial Activity of Wood Rotting Higher Basidiomycetes Mushrooms from Uruguay against Phytopathogens.

    Science.gov (United States)

    Barneche, Stephanie; Jorcin, Gabriela; Cecchetto, Gianna; Cerdeiras, María Pía; Vázquez, Alvaro; Alborés, Silvana

    2016-01-01

    In this work, the antimicrobial activity of extracts of wood rotting higher Basidiomycetes mushrooms isolated from Eucalyptus plantations in Uruguay was studied using bacterial and fungal phytopathogens as targets. Fifty-one extracts from mycelia and growth broth were prepared from higher Basidiomycetes mushrooms, from which eight extracts (from Ganoderma resinaceum, Laetiporus sulphureus, Dictyopanus pusillus, and Bjerkandera adusta) showed antimicrobial activity against Xanthomonas vesicatoria, Aspergillus oryzae, Penicillium expansum, Botrytis cinerea, and Rhizopus stolonifer as assayed in the qualitative test. The minimum inhibitory concentration (MIC) for those fungal extracts was determined and the results showed that L. sulphureus deserved further study, with low MIC values against X. vesicatoria. The antimicrobial activity of L. sulphureus culture broth extracts grown under different culture conditions was evaluated against X. vesicatoria. From the results of these assays, larger-scale cultures for the production of the compound(s) with antimicrobial activity should be performed using malt extract broth, at pH 5, at 20°C and static culture conditions. PMID:27481160

  19. Screening Neuropharmacological Activities of Kaempferia parviflora (Krachai Dam in Healthy Adult Male Rats

    Directory of Open Access Journals (Sweden)

    Thaneeya Hawiset

    2011-01-01

    Full Text Available Problem statement: Although the global prevalence of psychological disorders is increasing continually, the efficacies of therapeutic strategies are still very limited. Oxidative stress has been implicated in the pathogenesis of psychiatric disorders and substance possessing antioxidant activity can alleviate the mentioned conditions. Therefore, we hypothesized that Kaempferia parviflora, a medicinal plant claimed for nerve tonic, also possessed the neuropharmacological activities which provide the advantage for psychiatric disorders. Approach: Adult male Wistar rats, weighing 180-220 grams, were orally given the ethanolic extract of K. parviflora at doses of 150, 200 and 250 mg kg-1 BW once daily for 2 weeks. Then, they were determined the neuropharmacological activities including anxiolytic, anti-depression like behavior and cognitive enhancement after single dose, 1 and 2 weeks of treatment. Results: K. parviflora possessed anti-depression like behavior and cognitive enhancement at all treatment duration. Unfortunately, this substance failed to show anxiolytic like activity. Conclusion: Our results suggested that K. parviflora might be used as a novel therapeutic strategy for psychiatric disorder and cognitive enhancement. However, further investigations about precise underlying mechanism are still required.

  20. Screening of natural compounds as activators of the keap1-nrf2 pathway.

    Science.gov (United States)

    Wu, Kai C; McDonald, Peter R; Liu, Jie; Klaassen, Curtis D

    2014-01-01

    Nuclear factor erythroid 2-related factor 2 is a master regulator that promotes transcription of cytoprotective genes in response to oxidative/electrophilic stress. A large number of natural dietary compounds are thought to protect against oxidative stress, and a few have been reported to induce genes involved in antioxidant defense through activating nuclear factor erythroid 2-related factor 2. Therefore, a library of 54 natural compounds were collected to determine whether they are nuclear factor erythroid 2-related factor 2 activators and to compare their efficacy and potency to activate nuclear factor erythroid 2-related factor 2. The assay utilized AREc32 cells that contain a luciferase gene under the control of antioxidant response element promoters. Each natural compound was tested at 13 concentrations between 0.02 and 30 µM. Known nuclear factor erythroid 2-related factor 2 activators tert-butylhydroquinone and 2-cyano-3,12-dioxooleana-1,9-diene-28-imidazolide were used as positive controls in parallel with the natural compounds. Among the 54 tested natural compounds, andrographolide had the highest efficacy, followed by trans-chalcone, sulforaphane, curcumin, flavone, kahweol, and carnosol, all of which had better efficacy than tert-butylhydroquinone. Among the compounds tested, 2-cyano-3,12-dioxooleana-1,9-diene-28-imidazolide was the most potent, having an EC50 of 0.41 µM. Seven of the natural compounds, namely andrographolide, trans-chalcone, sulforaphane, curcumin, flavone, kahweol, and cafestol had lower EC50 values than tert-butylhydroquinone but higher than 2-cyano-3,12-dioxooleana-1,9-diene-28-imidazolide. The present study provides insights into which natural compounds activate the Keap1-nuclear factor erythroid 2-related factor 2 pathway and thus might be useful for detoxifying oxidative/electrophilic stress.

  1. Rapid screening and quantitative determination of bioactive compounds from fruit extracts of Myristica species and their in vitro antiproliferative activity.

    Science.gov (United States)

    Pandey, Renu; Mahar, Rohit; Hasanain, Mohammad; Shukla, Sanjeev K; Sarkar, Jayanta; Rameshkumar, K B; Kumar, Brijesh

    2016-11-15

    Efficient and sensitive LC-MS/MS methods have been developed for the rapid screening and determination of bioactive compounds in different fruit parts of four Myristica species, viz., Myristica beddomeii, Myristica fragrans, Myristica fatua and Myristica malabarica. Twenty-one compounds were identified and characterized on the basis of their accurate mass and MS/MS fragmentation pattern using HPLC-QTOF-MS/MS and NMR analysis. Quantitative determination of five major bioactive compounds was performed using multiple-reaction monitoring mode with continuous polarity switching by UHPLC-QqQLIT-MS/MS. Moreover, in vitro antiproliferative activity of these Myristica species was evaluated against five human cancer cell lines A549, DLD-1, DU145, FaDu and MCF-7 using SRB assay. Seventeen phytoconstituents were identified and reported for the first time from M. beddomeii and sixteen from M. fatua. Quantification result showed highest total content of five major bioactive compounds in mace of M. fragrans. Evaluation of in vitro antiproliferative activity revealed potent activity in all investigated species except M. fragrans. PMID:27283658

  2. Influence of different stool types on muscle activity and lumbar posture among dentists during a simulated dental screening task.

    Science.gov (United States)

    De Bruyne, Mieke A A; Van Renterghem, Benedikt; Baird, Andrew; Palmans, Tanneke; Danneels, Lieven; Dolphens, Mieke

    2016-09-01

    Whereas in the past dental stools typically facilitated a 90° hip angle, a number of currently available alternative designs allow for a more extended hip posture. The present study investigated the influence of different stool types on muscle activity and lumbar posture. Twenty five participants completed a simulated dental procedure on a standard stool, a saddle and the Ghopec. The latter stool comprises a seat pan consisting of a horizontal rear part for the pelvis and an inclinable sloping down front part for the upper legs, with a vertically and horizontally adjustable back rest. Lumbar posture was most close to neutral on the Ghopec, whereas sitting on a standard/saddle stool resulted in more flexed/extended postures respectively. Sitting with a 90° angle (standard stool) resulted in higher activation of back muscles while sitting with a 125° angle (saddle and Ghopec) activated abdominal muscles more, although less in the presence of a backrest (Ghopec). To maintain neutral posture during dental screening, the Ghopec is considered the most suitable design for the tasks undertaken. PMID:26975788

  3. M2 priority screening system for near-term activities: Project documentation. Final report December 11, 1992--May 31, 1994

    Energy Technology Data Exchange (ETDEWEB)

    NONE

    1993-08-12

    From May through August, 1993, the M-2 Group within M Division at LANL conducted with the support of the LANL Integration and Coordination Office (ICO) and Applied Decision Analysis, Inc. (ADA), whose purpose was to develop a system for setting priorities among activities. This phase of the project concentrated on prioritizing near-tenn activities (i.e., activities that must be conducted in the next six months) necessary for setting up this new group. Potential future project phases will concentrate on developing a tool for setting priorities and developing annual budgets for the group`s operations. The priority screening system designed to address the near-term problem was developed, applied in a series of meeting with the group managers, and used as an aid in the assignment of tasks to group members. The model was intended and used as a practical tool for documenting and explaining decisions about near-term priorities, and not as a substitute for M-2 management judgment and decision-making processes.

  4. Developing a rapid throughput screen for detection of nematicidal activity of plant cysteine proteinases: the role of Caenorhabditis elegans cystatins.

    Science.gov (United States)

    Phiri, A M; De Pomerai, D; Buttle, D J; Behnke, J M B

    2014-02-01

    Plant cysteine proteinases (CPs) from papaya (Carica papaya) are capable of killing parasitic nematode worms in vitro and have been shown to possess anthelmintic effects in vivo. The acute damage reported in gastrointestinal parasites has not been found in free-living nematodes such as Caenorhabditis elegans nor among the free-living stages of parasitic nematodes. This apparent difference in susceptibility might be the result of active production of cysteine proteinase inhibitors (such as cystatins) by the free-living stages or species. To test this possibility, a supernatant extract of refined papaya latex (PLS) with known active enzyme content was used. The effect on wild-type (Bristol N2) and cystatin null mutant (cpi-1(-/-) and cpi-2(-/-)) C. elegans was concentration-, temperature- and time-dependent. Cysteine proteinases digested the worm cuticle leading to release of internal structures and consequent death. Both cystatin null mutant strains were highly susceptible to PLS attack irrespective of the temperature and concentration of exposure, whereas wild-type N2 worms were generally resistant but far more susceptible to attack at low temperatures. PLS was able to induce elevated cpi-1 and cpi-2 cystatin expression. We conclude that wild-type C. elegans deploy cystatins CPI-1 and CPI-2 to resist CP attack. The results suggest that the cpi-1 or cpi-2 null mutants (or a double mutant combination of the two) could provide a cheap and effective rapid throughput C. elegans-based assay for screening plant CP extracts for anthelmintic activity.

  5. Screening of SDS-degrading Bacteria from Carwash Wastewater and the Study of the Alkylsulfatase Enzyme Activity

    Directory of Open Access Journals (Sweden)

    Razieh Shahbazi

    2013-06-01

    Full Text Available Background and Objectives: Sodium dodecyl sulfate (SDS is one of the main surfactant components in detergents and cosmetics, used in high amounts as a detergent in products such as shampoos, car wash soap and toothpaste. Therefore, its bioremediation by suitable microorganisms is important. Alkylsulfatase is an enzyme that hydrolyses sulfate -ester bonds to give inorganic sulfate and alcohol. The purpose of this study was to isolate SDS–degrading bacteria from Tehran city car wash wastewater, study bacterial alkylsulfatase enzyme activity and identify the alkylsulfatase enzyme coding gene.Materials and Methods: Screening of SDS-degrading bacteria was carried out on basal salt medium containing SDS as the sole source of carbon. Amount of SDS degraded was assayed by methylene blue active substance (MBAS.Results and Conclusion: Identification of the sdsA gene was carried by PCR and subsequent sequencing of the 16S rDNA gene and biochemical tests identified Pseudomonas aeruginosa. This bacterium is able to degrade 84% of SDS after four days incubation. Bacteria isolated from car wash wastewater were shown to carry the sdsA gene (670bp and the alkylsulfatase enzyme specific activity expressed from this gene was determined to be 24.3 unit/mg . The results presented in this research indicate that Pseudomonas aeruginosa is a suitable candidate for SDS biodegradation.

  6. Unbiased identification of signal-activated transcription factors by barcoded synthetic tandem repeat promoter screening (BC-STAR-PROM).

    Science.gov (United States)

    Gosselin, Pauline; Rando, Gianpaolo; Fleury-Olela, Fabienne; Schibler, Ueli

    2016-08-15

    The discovery of transcription factors (TFs) controlling pathways in health and disease is of paramount interest. We designed a widely applicable method, dubbed barcorded synthetic tandem repeat promoter screening (BC-STAR-PROM), to identify signal-activated TFs without any a priori knowledge about their properties. The BC-STAR-PROM library consists of ∼3000 luciferase expression vectors, each harboring a promoter (composed of six tandem repeats of synthetic random DNA) and an associated barcode of 20 base pairs (bp) within the 3' untranslated mRNA region. Together, the promoter sequences encompass >400,000 bp of random DNA, a sequence complexity sufficient to capture most TFs. Cells transfected with the library are exposed to a signal, and the mRNAs that it encodes are counted by next-generation sequencing of the barcodes. This allows the simultaneous activity tracking of each of the ∼3000 synthetic promoters in a single experiment. Here we establish proof of concept for BC-STAR-PROM by applying it to the identification of TFs induced by drugs affecting actin and tubulin cytoskeleton dynamics. BC-STAR-PROM revealed that serum response factor (SRF) is the only immediate early TF induced by both actin polymerization and microtubule depolymerization. Such changes in cytoskeleton dynamics are known to occur during the cell division cycle, and real-time bioluminescence microscopy indeed revealed cell-autonomous SRF-myocardin-related TF (MRTF) activity bouts in proliferating cells.

  7. Unbiased identification of signal-activated transcription factors by barcoded synthetic tandem repeat promoter screening (BC-STAR-PROM).

    Science.gov (United States)

    Gosselin, Pauline; Rando, Gianpaolo; Fleury-Olela, Fabienne; Schibler, Ueli

    2016-08-15

    The discovery of transcription factors (TFs) controlling pathways in health and disease is of paramount interest. We designed a widely applicable method, dubbed barcorded synthetic tandem repeat promoter screening (BC-STAR-PROM), to identify signal-activated TFs without any a priori knowledge about their properties. The BC-STAR-PROM library consists of ∼3000 luciferase expression vectors, each harboring a promoter (composed of six tandem repeats of synthetic random DNA) and an associated barcode of 20 base pairs (bp) within the 3' untranslated mRNA region. Together, the promoter sequences encompass >400,000 bp of random DNA, a sequence complexity sufficient to capture most TFs. Cells transfected with the library are exposed to a signal, and the mRNAs that it encodes are counted by next-generation sequencing of the barcodes. This allows the simultaneous activity tracking of each of the ∼3000 synthetic promoters in a single experiment. Here we establish proof of concept for BC-STAR-PROM by applying it to the identification of TFs induced by drugs affecting actin and tubulin cytoskeleton dynamics. BC-STAR-PROM revealed that serum response factor (SRF) is the only immediate early TF induced by both actin polymerization and microtubule depolymerization. Such changes in cytoskeleton dynamics are known to occur during the cell division cycle, and real-time bioluminescence microscopy indeed revealed cell-autonomous SRF-myocardin-related TF (MRTF) activity bouts in proliferating cells. PMID:27601530

  8. Phytochemical screening and antimicrobial activities of plant extract of Lantana camara.

    Science.gov (United States)

    Pradeep, B Vishwanath; Tejaswini, M; Nishal, P; Pardhu, G; Shylaja, S; Kumar, Kranthi Ch

    2013-05-01

    Natural products continue to play an important role in the discovery and development of new pharmaceuticals. Several chemical compounds have been extracted and identified from its species known as Lantana camara (L .camara). The present study was designed for phytochemical analysis of L. camara and extraction of bioactive compound by HPLC. This also included the antimicrobial activity of the bioactive compound obtained by crude extract and the column extract. The study showed the presence of the bioactive component parthenin extracted from the HPLC analysis at a peak height of 10.3807 and it was showing antimicrobial activity against E. coli, P. aeruginosa, B. subtilis and E. fecalis, crude (6.8 to 8.1 mm ) and column (4.0 to 6.2 mm) zone of inhibition. PMID:24617153

  9. Screening of the antimalarial activity of plants of the Cucurbitaceae family

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    Cláudia Zuany Amorim

    1991-01-01

    Full Text Available Crude ethanolic extracts (CEEs from two species of Cucurbitaceae, Cucurbita maxima and Momordica charantia (commonly called "abóbora moranga" and melão de São Caetano", respectively were assayed for antimalarial activity by the 4-d suppressive test. The CEE of dry C. maxima seeds showed strong antimalarial activity following oral administration (259 and 500 mg/kg, reducing by 50% the levels of parasistemia in Plasmodium berghey-infected mice. Treatment of normal animals with 500 mg/Kg of the extract three days before intravenous injection of P. berghei caused a significant 30% reduction in parasitemic levels. No effect was observed when the animals were treated with the CEE only on the day of inoculation. Oral administration of the CEE of dry M. charantia leaves adminstered orally was ineffective up to 500 mg/Kg in lowering the parasitemic levels of malarious mice.

  10. SCREENING OF THE ANTIINFLAMMATORY ACTIVITY OF “TRIANTHEMA PORTULACASTRUM” IN ACUTE MODELS OF INFLAMMATION

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    Suresh S

    2015-04-01

    Full Text Available BACKGROUND : There are many anti - inflammatory drugs available but all of them do have a significant adverse effect profile. Trianthema portulacastrum is known in Ayurveda since centuries for its medicinal values. So the current study was underta ken to evaluate the anti - inflammatory effects of this plant in acute inflammation. MATERIALS AND METHOD S : Albino rats were treated with whole plant ethonolic extract of Trianthema portulacastrum 100mg \\ kg, indomethacin 20 mg \\ kg, orally with 2% gum acacia as suspending agent and the effects were observed in acute models of inflammation viz, carrrageenin induced paw edema and formalin induced peritonitis. RESULTS : our study demonstrated that Trianthema portulacastrum exhibited significant anti - inflammatory activity in both the models. CONCLUSION : Trianthema potrulacastum has got significant anti - inflammatory activity so further studies are needed in this direction.

  11. Screening of Antimicrobial activity of Aqueous extracts of Leaves, Flower and Stem of Eclipta alba

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    Prabhsimran Singh Sandhu

    2012-12-01

    Full Text Available Plants are the oldest source of pharmacologically active compounds, and have provided humankind with many medically useful compounds for centuries. In this study aqueous extract of leaves, stem and flower of Eclipta alba were tested for antimicrobial activity against Escherichia coli (ATCC25923,Enterobacter cloacae (ATCC10699, Enterococcus faecalis (ATCC10741, Proteus vulgaris (ATCC12454 Staphylococcus aureus (ATCC25923 Klebsiella pneumonia (ATCC15380 and Staphylococcus. Saprophyticus (ATCC35552 It was shown that leaves extract effective against E. cloacae & K .pneumoniae but not against others, while aquous extract of stem shown good antitimicrobial effect against E. cloacae, E. faecali, K. pneumoniae and S. saprophyticus but E. coli, P. vulgaris, S. aureus were found resistant and The aqueous extract of flower shown reliabe ZOI against P.vulgaris ,S.aureus and S.saprophyticus while resistant against all other microbes.

  12. Screening of chemical composition, antimicrobial and antioxidant activities of Artemisia essential oils.

    Science.gov (United States)

    Lopes-Lutz, Daíse; Alviano, Daniela S; Alviano, Celuta S; Kolodziejczyk, Paul P

    2008-05-01

    The chemical composition of essential oils isolated from aerial parts of seven wild sages from Western Canada -Artemisia absinthium L., Artemisia biennis Willd., Artemisia cana Pursh, Artemisia dracunculus L., Artemisia frigida Willd., Artemisia longifolia Nutt. and Artemisia ludoviciana Nutt., was investigated by GC-MS. A total of 110 components were identified accounting for 71.0-98.8% of the oil composition. High contents of 1,8-cineole (21.5-27.6%) and camphor (15.9-37.3%) were found in Artemisia cana, A. frigida, A. longifolia and A. ludoviciana oils. The oil of A. ludoviciana was also characterized by a high content of oxygenated sesquiterpenes with a 5-ethenyltetrahydro-5-methyl-2-furanyl moiety, of which davanone (11.5%) was the main component identified. A. absinthium oil was characterized by high amounts of myrcene (10.8%), trans-thujone (10.1%) and trans-sabinyl acetate (26.4%). A. biennis yielded an oil rich in (Z)-beta-ocimene (34.7%), (E)-beta-farnesene (40.0%) and the acetylenes (11.0%) (Z)- and (E)-en-yn-dicycloethers. A. dracunculus oil contained predominantly phenylpropanoids such as methyl chavicol (16.2%) and methyl eugenol (35.8%). Artemisia oils had inhibitory effects on the growth of bacteria (Escherichia coli, Staphylococcus aureus, and Staphylococcus epidermidis), yeasts (Candida albicans, Cryptococcus neoformans), dermatophytes (Trichophyton rubrum, Microsporum canis, and Microsporum gypseum), Fonsecaea pedrosoi and Aspergillus niger. A. biennis oil was the most active against dermatophytes, Cryptococcus neoformans, Fonsecaea pedrosoi and Aspergillus niger, and A. absinthium oil the most active against Staphylococcus strains. In addition, antioxidant (beta-carotene/linoleate model) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activities were determined, and weak activities were found for these oils. PMID:18417176

  13. Preliminary Screening of Tinospora cordifolia Extracts and Guduchi Satva for Anti-Rheumatoid Activity

    OpenAIRE

    Shah Palak A.; Shah Gaurang B.

    2016-01-01

    Extracts of Tinospora cordifolia viz. aqueous (TCA), hydroalcoholic (TCH), dichloromethane (TCD) extracts and guduchi satva (TCP) (starch), were studied for anti-rheumatoid activity in complete freund’s adjuvant (CFA) induced rheumatoid arthritis (RA). Female albino Wistar rats (body weight: 170 to 200 g) were divided in 11 groups each containing 3 animals. RA was induced by injecting CFA in sub plantar region of left paw in all animals (day 0) except Group I (normal control). Group II (dise...

  14. Phytochemical screening of five medicinal legumes and their evaluation for in vitro anti-tubercular activity

    OpenAIRE

    Kumar, J. Komal; Devi Prasad, A. G.; Chaturvedi, Vinita

    2014-01-01

    Background: Tuberculosis is a leading cause of death in the world. A new alternative for the treatment of tuberculosis is urgently required, due to the emergence of multidrug resistant Mycobacterium tuberculosis. Aim: There is currently considerable interest in developing potential drugs from medicinal plants for treating tuberculosis. To evaluate anti-tubercular activity in the leaves of Kingiodendron pinnatum Rox. Hams., Humboldtia brunonis Wall., Indigofera cassioides Rottl.ex DC., Derris ...

  15. Screening of Psidium guajava Leaf Extracts for Antistress Activity in Different Experimental Animal Models

    OpenAIRE

    Lakshmi, B. V. S.; Sudhakar, M.

    2009-01-01

    Ethanolic extract of leaves of Psidium guajava was investigated on anoxia stress tolerance test in Swiss mice. The animals were also subjected to acute physical stress (swimming endurance test) and acute heat induced stress to gauge the antistress potential of the extract. Further to evaluate the antistress activity of Psidium guajava in chronic stress condition, fresh Wistar rats were subjected to cold restraint stress (4° for 2 h) for 10 days. Stimulation of hypothalamus pituitary adrenal a...

  16. Experiences of counselling on physical activity during pregnancy Gestational diabetes mellitus : screening and pregnancy outcomes

    OpenAIRE

    Lindqvist, Maria

    2016-01-01

    Background Overweight and obesity are global health problems with several adverse health effects that threaten public health. In Sweden, almost four of ten pregnant women are overweight or obese, conditions that are associated with adverse pregnancy outcomes, including gestational diabetes mellitus (GDM), a metabolic disorder that complicates pregnancy. Globally, physical inactivity is the fourth leading risk factor for mortality. The recommendation for physical activity (i.e., ≥150 minutes/w...

  17. SCREENING OF IN-VITRO ANTHELMENTIC ACTIVITY OF KALANCHOE PINNATA ROOTS

    OpenAIRE

    Quazi Majaz A.; Sayyed Nazim; Quazi Asir; Quazi Shoeb; Gulati M. Bilal

    2011-01-01

    The plant Kalanchoe pinnata is widely used in ayurvedic system of medicine as astringent, analgesic, carminative and also useful in diarrhea and vomiting. Naturalized throughout the hot and moist parts of India. In this first roots are subjected to pet.ether, chloroform, methanol and aqueous solvent respectively for extraction. And the in vitro evaluation of anthelmentic activity was done against Pheretima posthuma (Annelida), Ascardia galli (nematode). Methanolic extract of roots of K. pinna...

  18. Activity-guided screening of the antioxidants from Paulownia tomentosa var. tomentosa Bark

    OpenAIRE

    Chuan-Ling Si; Shi-Chao Liu; Hai-Yan Hu; Ju-Zheng Jiang; Guo-Jing Yu; Xiao-Dan Ren; Guang-Hui Xu

    2013-01-01

    Tree barks, as a type of forestry residues, are a rich and renewable bioresource that can produce high value-added products. Paulownia tomentosa var. tomentosa (PTT) has been extensively used in traditional Chinese medicine to cure various diseases. However, the antioxidative activity of the chemical constituents of the tree has not yet been investigated. In this study, the bark of PTT were extracted and fractioned. Then the resulting ethyl acetate (EtOAc) soluble fraction, which exhibited th...

  19. Quantitative Brain Electrical Activity in the Initial Screening of Mild Traumatic Brain Injuries

    OpenAIRE

    O'Neil, Brian; Prichep, Leslie S.; Naunheim, Roseanne; Chabot, Robert

    2012-01-01

    Introduction: The incidence of emergency department (ED) visits for Traumatic Brain Injury (TBI) in the United States exceeds 1,000,000 cases/year with the vast majority classified as mild (mTBI). Using existing computed tomography (CT) decision rules for selecting patients to be referred for CT, such as the New Orleans Criteria (NOC), approximately 70% of those scanned are found to have a negative CT. This study investigates the use of quantified brain electrical activity to assess its possi...

  20. Activity screening of plant growth promoting rhizobacteria isolated from alfalfa rhizosphere

    OpenAIRE

    shahla pashapour; Hossein besharati; Mahmoud rezazadeh; Ahmad Alimadadi; Nadergholi Ebrahimi

    2016-01-01

    Introduction: Some rhizobacteria by various mechanisms influence plant growth as they are called plant growth promoting rhizobacteria (PGPR). Scientists identified some PGPR characters involved in promoting plant growth, while all these characters are not able to study. The aim of this study was to evaluate PGP activities of bacterial isolates, (45 isolates belonged to rhizobium and 2 bacterial isolates belonged to Pseudomonas fluorescens), which were isolated from alfalfa (Medicago sativa) r...

  1. Chemical constituents from Tribulus terrestris and screening of their antioxidant activity.

    Science.gov (United States)

    Hammoda, Hala M; Ghazy, Nabila M; Harraz, Fathalla M; Radwan, Mohamed M; ElSohly, Mahmoud A; Abdallah, Ingy I

    2013-08-01

    Two oligosaccharides (1,2) and a stereoisomer of di-p-coumaroylquinic acid (3) were isolated from the aerial parts of Tribulus terrestris along with five known compounds (4-8). The structures of the compounds were established as O-β-D-fructofuranosyl-(2→6)-α-D-glucopyranosyl-(1→6)-β-D-fructofuranosyl-(2→6)-β-D-fructofuranosyl-(2→1)-α-D-glucopyranosyl-(6→2)-β-D-fructofuranoside (1), O-α-D-glucopyranosyl-(1→4)-α-D-glucopyranosyl-(1→4)-α-D-glucopyranosyl-(1→2)-β-D-fructofuranoside (2), 4,5-di-p-cis-coumaroylquinic acid (3) by different spectroscopic methods including 1D NMR ((1)H, (13)C and DEPT) and 2D NMR (COSY, TOCSY, HMQC and HMBC) experiments as well as ESI-MS analysis. This is the first report for the complete NMR spectral data of the known 4,5-di-p-trans-coumaroylquinic acid (4). The antioxidant activity represented as DPPH free radical scavenging activity was investigated revealing that the di-p-coumaroylquinic acid derivatives possess potent antioxidant activity so considered the major constituents contributing to the antioxidant effect of the plant. PMID:23642392

  2. ANTIMICROBIAL ACTIVITY AND PHYTOCHEMICAL SCREENING OF FRESH LATEX OF EUPHORBIA THYMIFOLIA LINN

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    Killedar Suresh Ganpati

    2011-05-01

    Full Text Available Euphorbia thymifolia Linn is small branched, pubescent, prostate annual herb with opposite oblong leaves, commonly known as laghududhika or choti-dudhi. Plant juice is employed in south India as cure for ring worms. The ethyl acetate extract and chloroform extract is reported to inhibit the growth of E. coli and Shigella flexneri. No scientific literature was found on medicinal properties of fresh latex. Hence the present work was designed to evaluate the traditional claims of Euphorbia thymifolia Linn. We have collected the fresh latex of plant by capillary action (1 kg of fresh sample gives 1.5ml of latex. The collected fresh latex was tested for antimicrobial activity by cylindrical cup plate method using standard cultures. Fresh latex showed maximum activity compare to diluted latex, dried latex, fresh juice and ethyl acetate, butanol, chloroform extracts of fresh plant. The antimicrobial activity of latex was found comparable with ciprofloxacin and fluconazole at tested concentration. The latex showed presence of tannins, resins, glycosides and sugars.

  3. Coccoloba uvifera (L. (Polygonaceae Fruit: Phytochemical Screening and Potential Antioxidant Activity

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    Maira Rubi Segura Campos

    2015-01-01

    Full Text Available The flora of Latin America attracts gaining interest as it provides a plethora of still unexplored or underutilized fruits that can contribute to human well-being due to their nutritional value and their content of bioactive compounds. Antioxidant compounds are now of considerable interest due to their effect of preventing or delaying aging and their apparent involvement in prevention of numerous human diseases, including cancer, atherosclerosis, Alzheimer’s disease, inflammation, and rheumatoid arthritis. In this work, the fruit of Coccoloba uvifera (L. was investigated for their in vitro antioxidant capacity using two assays based on reactions with a relatively stable single reagent radical (Trolox equivalent antioxidant capacity, TEAC; and DPPH free radical scavenging assay, DPPH, two assays based on chelating of metallic cations, and one based on the reduction of oxidized species. The TEAC value on ABTS radical, DPPH scavenging activity, ion chelation, and reducing power were found to be 897.6 μM of Trolox/100 g of sample, 22.8% of DPPH free radical scavenging, 11.3% of Cu2+-chelating activity, 23.9% of Fe2+-chelating activity, and a Fe2+-reducing power of 0.76 mg/mL, respectively. The free radical scavenging and antioxidant characteristics of C. uvifera may be due to the presence of diverse phytochemicals in the fruit as anthocyanins, ascorbic acid, phenolic compounds, and flavonoids.

  4. SCREENING OF THE ANTIBACTERIAL ACTIVITY OF AMORPHOPHALLUS CAMPANULATUS FROM BASTAR REGION OF CHHATTISGARH, INDIA

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    Dhananjay Pandey

    2013-12-01

    Full Text Available The present study was aimed to evaluate the antibacterial activity of Amorphophallus campanulatus (family: Araceae commonly known as jangli suran. The root, stem and leaf of A. campanulatus, extracted successively with polar (aqueous, methanol, dipolar (acetone and non polar (chloroform solvents, yielded more phyto compounds in case of root followed by stem and leaf. The extracts were assessed for their antibacterial activity against both gram positive and gram negative bacteria viz., Bacillus cerus, Bacillus subtilis, Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli, Proteus vulgaris, Pseudomonas aeruginosa and Klebsiella pneumoneae. The gram positive bacteria were found to be more sensitive than gram negative bacteria. The inhibition of both gram positive and gram negative bacteria by the extracts indicate the presence of broad spectrum antibiotic potential. The root extract of the plant was found to be more effective in inhibiting the bacterial growth as compared to stem and leaf. The methanol root extract of the plant showed maximum inhibition against all gram positive and one gram negative Pseudomonas aeruginosa bacteria followed by acetone and chloroform. The highest activity index was recorded in methanol extract of root in Pseudomonas aeruginosa. The results were promising and supported the use of plants root by traditional healers in curing several ailments.

  5. SCREENING FOR ANTI ULCER ACTIVITY OF CONVOLVULUS PLURICAULIS USING PYLORIC LIGATION METHOD IN WISTER RATS.

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    Sharath S S

    2015-01-01

    Full Text Available Peptic ulcer disease is a chronic problem of the gastrointestinal tract characterized by mucosal damage secondary to pepsin and gastric acid secretion. Herbal medicines are generally used in cases when drugs are to be used for chronic periods. The study was conducted to evaluate antiulcerogenic activity of convolvulus pluricaulis in wistar rats. The antiulcer activity was carried out employing - Pyloric ligation method. The rats were randomly divided into 4 groups of 6 animals each. First group was given 1ml of 0.1% of vehicle (Tween 80; the second group was treated with ranitidine 50 mg/kg in 1 ml Tween 80. The remaining groups receive 200 mg/kg and 400 mg/kg of Convolvulus pluricaulis alcoholic extract (CPAE in 1 ml Tween 80 respectively. All the drugs were administered orally for five days duration daily in two divided doses. Evaluation of antiulcer activity was done by Ulcer score/ulcer index. Volume of gastric juice secreted, gastric free acidity, total acidity, total protein, pepsin mucin and pH were also estimated. CPAE at a dose of 200 mg/kg inhibited ulcer index by 40.87% and at a dose of 400 mg/kg inhibited ulcer index by 26.64 %. Alcoholic extracts of Convolvulus pluricaulis have shown a significant protection against gastric ulcers in pyloric ligation model.

  6. Bioactivity screening of microalgae for antioxidant, anti-inflammatory, anticancer, anti-diabetes and antibacterial activities

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    Chiara eLauritano

    2016-05-01

    Full Text Available Marine microalgae are considered a potentially new and valuable source of biologically active molecules for applications in the food industry as well as in the pharmaceutical, nutraceutical and cosmetic sectors. They can be easily cultured, have short generation times and enable an environmentally-friendly approach to drug discovery by overcoming problems associated with the over-utilization of marine resources and the use of destructive collection practices. In this study, 21 diatoms, 7 dinoflagellates and 4 flagellate species were grown in three different culturing conditions and the corresponding extracts were tested for possible antioxidant, anti-inflammatory, anticancer, anti-diabetes, antibacterial and anti-biofilm activities. In addition, for two diatoms we also tested two different clones to disclose diversity in clone bioactivity. Six diatom species displayed specific anti-inflammatory, anticancer (blocking human melanoma cell proliferation and anti-biofilm (against the bacteria Staphylococcus epidermidis activities whereas, none of the other microalgae were bioactive against the conditions tested for. Furthermore, none of the 6 diatom species tested were toxic on normal human cells. Culturing conditions (i.e. nutrient starvation conditions greatly influenced bioactivity of the majority of the clones/species tested. This study denotes the potential of diatoms as sources of promising bioactives for the treatment of human pathologies.

  7. Reactive Oxygen Species (ROS)-Activated ATM-Dependent Phosphorylation of Cytoplasmic Substrates Identified by Large-Scale Phosphoproteomics Screen.

    Science.gov (United States)

    Kozlov, Sergei V; Waardenberg, Ashley J; Engholm-Keller, Kasper; Arthur, Jonathan W; Graham, Mark E; Lavin, Martin

    2016-03-01

    Ataxia-telangiectasia, mutated (ATM) protein plays a central role in phosphorylating a network of proteins in response to DNA damage. These proteins function in signaling pathways designed to maintain the stability of the genome and minimize the risk of disease by controlling cell cycle checkpoints, initiating DNA repair, and regulating gene expression. ATM kinase can be activated by a variety of stimuli, including oxidative stress. Here, we confirmed activation of cytoplasmic ATM by autophosphorylation at multiple sites. Then we employed a global quantitative phosphoproteomics approach to identify cytoplasmic proteins altered in their phosphorylation state in control and ataxia-telangiectasia (A-T) cells in response to oxidative damage. We demonstrated that ATM was activated by oxidative damage in the cytoplasm as well as in the nucleus and identified a total of 9,833 phosphorylation sites, including 6,686 high-confidence sites mapping to 2,536 unique proteins. A total of 62 differentially phosphorylated peptides were identified; of these, 43 were phosphorylated in control but not in A-T cells, and 19 varied in their level of phosphorylation. Motif enrichment analysis of phosphopeptides revealed that consensus ATM serine glutamine sites were overrepresented. When considering phosphorylation events, only observed in control cells (not observed in A-T cells), with predicted ATM sites phosphoSerine/phosphoThreonine glutamine, we narrowed this list to 11 candidate ATM-dependent cytoplasmic proteins. Two of these 11 were previously described as ATM substrates (HMGA1 and UIMCI/RAP80), another five were identified in a whole cell extract phosphoproteomic screens, and the remaining four proteins had not been identified previously in DNA damage response screens. We validated the phosphorylation of three of these proteins (oxidative stress responsive 1 (OSR1), HDGF, and ccdc82) as ATM dependent after H2O2 exposure, and another protein (S100A11) demonstrated ATM

  8. Systematic screening of plant extracts from the Brazilian Pantanal with antimicrobial activity against bacteria with cariogenic relevance.

    Science.gov (United States)

    Brighenti, F L; Salvador, M J; Delbem, Alberto Carlos Botazzo; Delbem, Ádina Cleia Bottazzo; Oliveira, M A C; Soares, C P; Freitas, L S F; Koga-Ito, C Y

    2014-01-01

    This study proposes a bioprospection methodology regarding the antimicrobial potential of plant extracts against bacteria with cariogenic relevance. Sixty extracts were obtained from ten plants--(1) Jatropha weddelliana, (2) Attalea phalerata, (3) Buchenavia tomentosa, (4) Croton doctoris, (5) Mouriri elliptica, (6) Mascagnia benthamiana, (7) Senna aculeata, (8) Unonopsis guatterioides, (9) Allagoptera leucocalyx and (10) Bactris glaucescens--using different extraction methods - (A) 70° ethanol 72 h/25°C, (B) water 5 min/100°C, (C) water 1 h/55°C, (D) water 72 h/25°C, (E) hexane 72 h/25°C and (F) 90° ethanol 72 h/25°C. The plants were screened for antibacterial activity at 50 mg/ml using the agar well diffusion test against Actinomyces naeslundii ATCC 19039, Lactobacillus acidophilus ATCC 4356, Streptococcus gordonii ATCC 10558, Streptococcus mutans ATCC 35688, Streptococcus sanguinis ATCC 10556, Streptococcus sobrinus ATCC 33478 and Streptococcus mitis ATCC 9811. The active extracts were tested to determine their minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC), cytotoxicity and chemical characterization. Forty-seven extracts (78%) were active against at least one microorganism. Extract 4A demonstrated the lowest MIC and MBC for all microorganisms except S. gordonii and the extract at MIC concentration was non-cytotoxic. The concentrated extracts were slightly cytotoxic. Electrospray ionization with tandem mass spectrometry analyses demonstrated that the extract constituents coincided with the mass of the terpenoids and phenolics. Overall, the best results were obtained for extraction methods A, B and C. The present work proved the antimicrobial activity of several plants. Particularly, extracts from C. doctoris were the most active against bacteria involved in dental caries disease. PMID:24603299

  9. Wild Sicilian rosemary: phytochemical and morphological screening and antioxidant activity evaluation of extracts and essential oils.

    Science.gov (United States)

    Napoli, Edoardo M; Siracusa, Laura; Saija, Antonella; Speciale, Antonio; Trombetta, Domenico; Tuttolomondo, Teresa; La Bella, Salvatore; Licata, Mario; Virga, Giuseppe; Leone, Raffaele; Leto, Claudio; Rubino, Laura; Ruberto, Giuseppe

    2015-07-01

    To identify the best biotypes, an extensive survey of Sicilian wild rosemary was carried out by collecting 57 samples from various sites, followed by taxonomic characterization from an agronomic perspective. All the biotypes collected were classified as Rosmarinus officinalis L. A cluster analysis based on the morphological characteristics of the plants allowed the division of the biotypes into seven main groups, although the characteristics examined were found to be highly similar and not area-dependent. Moreover, all samples were analyzed for their phytochemical content, applying an extraction protocol to obtain the nonvolatile components and hydrodistillation to collect the essential oils for the volatile components. The extracts were characterized by LC-UV-DAD/ESI-MS, and the essential oils by GC-FID and GC/MS analyses. In the nonvolatile fractions, 18 components were identified, namely, 13 flavones, two organic acids, and three diterpenes. In the volatile fractions, a total of 82 components were found, with as predominant components α-pinene and camphene among the monoterpene hydrocarbons and 1,8-cineole, camphor, borneol, and verbenone among the oxygenated monoterpenes. Cluster analyses were carried out on both phytochemical profiles, allowing the separation of the rosemary samples into different chemical groups. Finally, the total phenol content and the antioxidant activity of the essential oils and extracts were determined with the Folin-Ciocalteu (FC) colorimetric assay, the UV radiation-induced peroxidation in liposomal membranes (UV-IP test), and the scavenging activity of the superoxide radical (O$\\rm{{_{2}^{{^\\cdot} -}}}$). The present study confirmed that the essential oils and organic extracts of the Sicilian rosemary samples analyzed showed a considerable antioxidant/free radical-scavenging activity. PMID:26172328

  10. Wild Sicilian rosemary: phytochemical and morphological screening and antioxidant activity evaluation of extracts and essential oils.

    Science.gov (United States)

    Napoli, Edoardo M; Siracusa, Laura; Saija, Antonella; Speciale, Antonio; Trombetta, Domenico; Tuttolomondo, Teresa; La Bella, Salvatore; Licata, Mario; Virga, Giuseppe; Leone, Raffaele; Leto, Claudio; Rubino, Laura; Ruberto, Giuseppe

    2015-07-01

    To identify the best biotypes, an extensive survey of Sicilian wild rosemary was carried out by collecting 57 samples from various sites, followed by taxonomic characterization from an agronomic perspective. All the biotypes collected were classified as Rosmarinus officinalis L. A cluster analysis based on the morphological characteristics of the plants allowed the division of the biotypes into seven main groups, although the characteristics examined were found to be highly similar and not area-dependent. Moreover, all samples were analyzed for their phytochemical content, applying an extraction protocol to obtain the nonvolatile components and hydrodistillation to collect the essential oils for the volatile components. The extracts were characterized by LC-UV-DAD/ESI-MS, and the essential oils by GC-FID and GC/MS analyses. In the nonvolatile fractions, 18 components were identified, namely, 13 flavones, two organic acids, and three diterpenes. In the volatile fractions, a total of 82 components were found, with as predominant components α-pinene and camphene among the monoterpene hydrocarbons and 1,8-cineole, camphor, borneol, and verbenone among the oxygenated monoterpenes. Cluster analyses were carried out on both phytochemical profiles, allowing the separation of the rosemary samples into different chemical groups. Finally, the total phenol content and the antioxidant activity of the essential oils and extracts were determined with the Folin-Ciocalteu (FC) colorimetric assay, the UV radiation-induced peroxidation in liposomal membranes (UV-IP test), and the scavenging activity of the superoxide radical (O$\\rm{{_{2}^{{^\\cdot} -}}}$). The present study confirmed that the essential oils and organic extracts of the Sicilian rosemary samples analyzed showed a considerable antioxidant/free radical-scavenging activity.

  11. Screening Antimicrobial Activity of Nickel Nanoparticles Synthesized Using Ocimum sanctum Leaf Extract

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    Chitra Jeyaraj Pandian

    2016-01-01

    Full Text Available Antimicrobial efficacy of nickel nanoparticles synthesized using leaf extract of Ocimum sanctum (NiGs was investigated against pathogenic Gram-negative (E. coli, K. pneumoniae, and S. typhi, Gram-positive (B. subtilis, S. epidermidis bacteria and fungi (C. albicans, C. tropicalis, A. fumigatus, A. clavatus, and A. niger. 100 µg/mL NiGs showed maximum antimicrobial activity against tested pathogens compared to leaf extract and antibiotics. E. coli (25 mm and C. albicans (23 mm exhibited higher zone of inhibition at 100 µg/mL NiGs. MIC, MBC, and MFC values of NiGs against all tested pathogens ranged between 25 and 50 µg/mL. Growth of bacterial and fungal cells (105 cfu/mL was completely inhibited at 50 µg/mL NiGs. E. coli and C. albicans have showed strong antimicrobial activity with 81% and 50% reactive oxygen species (ROS production, 30 and 16 µg/mL protein leakage, and 95 and 82 U/L LDH leakages, respectively. Gram-negative bacteria and Candida species showed more sensitivity to NiGs at all concentrations tested (25–100 µg/mL than Gram-positive bacteria and Aspergillus species, respectively. Microbial growth in the presence of NiGs and ascorbic acid confirmed the involvement of ROS in antimicrobial activity. Hence, NiGs induced ROS generation was attributed to the protein and LDH leakage from microbial membranes.

  12. Phytochemical Screening and In vitro Evaluation of Free Radical Scavenging Activity of Dionysia revoluta L.

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    Mohammad Ali Farboodniay Jahromi

    2015-03-01

    Full Text Available Dionysia revoluta L., a plant of Primulaceae family is used for treating ulcers and relieving pain in Iranian traditional system of medicine. The present study was aimed at preliminary phytochemical investigation and evaluation of antioxidant characteristics of D. revolute L. ethanol extract and its various fractions. Total phenolic content was determined by Folin–Ciocalteu method. Evaluation of total flavonoid was carried out by the use of an aluminium chloride/sodium carbonate colorimetric procedure. Lipid peroxidation inhibitory effect of ethanol extract was studied and compared with that of butylated hydroxytoluene (BHT. Radical scavenging properties of ethanolic extract and various fractions were determined by 2,2-diphenyl-l-picrylhydrazyl (DPPH and nitric oxide methods. High phenolic and flavonoid contents and significant radical scavenging properties were detected for the ethyl, acetate and n-butanol fractions. Comparisons were made with known reference antioxidant compounds ascorbic acid, quercetin, and gallic acid. The radical scavenging effect of n-butanol fraction was the highest among all fractions. Acid hydrolysis of n-butanol fraction led to a significant enhancement in its phenolic and flavonoid contents and DPPH scavenging efficacy. The total phenolic content showed a good correlation with radical scavenging activity. The antioxidant activity found in the ethyl acetate and n-butanol fractions of D. revoluta L. may be attributed to the presence of flavonoids and other phenolic compounds. Among various chemical constituents of this plant, the concentration of flavonoids seems to prevail remarkably as indicated by thin layer chromatography of various fractions and diagnostic colour reactions. The results suggest that D. revoluta bears a remarkable radical scavenging and antioxidant activity and is worthy of further detailed phytochemical and antioxidant studies.

  13. Screening of the target genes trans-activated by HLA-HA8 in hepatocytes

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    Qi WANG

    2011-06-01

    Full Text Available Objective To clone and identify the target genes trans-activated by human minor histocompatibility antigen HLA-HA8 in hepatocytes with suppression subtractive hybridization(SSH and bioinfomatics technique.Methods mRNA was isolated from HepG2 cells transfected by pcDNA3.1(--HLA-HA8 and pcDNA3.1(- empty vector,and then used to synthesize the double-stranded cDNA(marked as Tester and Driver,respectively by reverse transcription.After being digested with restriction enzyme Rsa I,the tester cDNA was divided into two parts and ligated to the specific adaptor 1 and adaptor 2,respectively,and then hybridized with driver cDNA twice and underwent PCR twice.The production was subcloned into pEGM-Teasy plasmid vectors to set up the subtractive library.The library was then amplified by transfection into E.coli strain DH5α.The cDNA was sequenced and analyzed in GenBank with Blast search after PCR amplification.Results The subtractive library of genes trans-activated by HLA-HA8 was constructed successfully.The amplified library contained 101 positive clones.Colony PCR showed that all these clones contained 200-1000bp inserts.Twenty eight clones were selected randomly to analyze the sequences.The result of homologous analysis showed that altogether 16 coding sequences were gotten,of which 4 sequences were with unknown function.Conclusions The obtained sequences trans-activated by HLA-HA8 may code different proteins and play important roles in cell growth and metabolism,energy synthesis and metabolism,material transport and signal transduction.This finding will bring some new clues for the studies not only on the biological functions of HLA-HA8,but also on the HBV infection mechanism.

  14. Screening for hemostatic activities of popular Chinese medicinal herbs in vitro

    OpenAIRE

    Naoki Ohkura; Haruna Yokouchi; Mariyo Mimura; Riki Nakamura; Gen-ichi Atsumi

    2015-01-01

    Aims The present study aimed to identify new hemostyptics by assessing the coagulation enhancing activity of 117 Chinese herbal extracts in vitro. Methods Herbs were boiled in water for about 30 min, filtered and then lyophilized filtrates (10 mg/mL) were dissolved in water. Coagulation was assayed as prothrombin time (PT). Plasma diluted in saline was incubated with each extract for five minutes and then PT reagent was added followed by CaCl2 solution and the time taken to form ...

  15. In vitro Screening of Essential Oil Active Compounds for Manipulation of Rumen Fermentation and Methane Mitigation

    OpenAIRE

    Joch, M.; Cermak, L.; Hakl, J.; Hucko, B.; Duskova, D.; Marounek, M.

    2015-01-01

    The objective of this study was to investigate the effects of 11 active compounds of essential oils (ACEO) on rumen fermentation characteristics and methane production. Two trials were conducted. In trial 1, ACEO (eugenol, carvacrol, citral, limonene, 1,4-cineole, p-cymene, linalool, bornyl acetate, α-pinene, and β-pinene) at a dose of 1,000 μL/L were incubated for 24 h in diluted rumen fluid with a 70:30 forage:concentrate substrate (16.2% crude protein; 36.6% neutral detergent fiber). Three...

  16. Screening, Identification and Antibacterial Activities of Effective Thermotolerant Bacillus spp. Strains Isolated from Raw Milk

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    Kannikar SANTONG

    2008-01-01

    Full Text Available Forty-one isolates of Bacillus species were isolated from raw milk, analyzed using the spot on lawn and agar diffusion method in terms of their general inhibition effects to test bacteria (Escherichia coli TISTR 887 and Staphylococcus aureus TISTR 517. The results demonstrated that most isolates are effective against Gram-positive and Gram-negative bacteria whereas their extensive inhibition effect is particularly against Gram-positive bacteria. Only 2 effective thermotolerant isolates, BA8 and BA16, exerted broad spectrum antibacterial activities against both test bacteria.  Based on biochemical and physiological properties, they were classified as Brevibacillus laterosporus and Geobacillus thermoglucosidasius, respectively.

  17. [Screening of phagocyte activators in plants; enhancement of TNF production by flavonoids].

    Science.gov (United States)

    Kunizane, H; Ueda, H; Yamazaki, M

    1995-09-01

    The tumor necrosis factor (TNF) was first discovered as a substance that induced necrosis of transplanted tumors. Recently, TNF has been recognized as an important and endogenous mediator in host defense mechanisms. To prove the fact that plant foods contain substances which activate the host defense mechanisms, we first examined if the administration of flavonoids could induce TNF production in mice. Some selected flavonoids such as naringin, apiin, poncirin and rutin were shown to amplify TNF release from murine macrophages in vivo in response to OK-432 as a second stimulus. However, their aglycone forms were not effective. The differences in the saccharide-chain of flavonoids induced the variety of TNF production.

  18. PHYTOCHEMICAL SCREENING OF AQUEOUS EXTRACT OF Piper betel LEAVES FOR ANTIBACTERIAL ACTIVITY

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    GOPALGHARE DIPALI

    2015-03-01

    Full Text Available Plants can be extracted and used for research work and are known to produce and store many Biochemical products. Different types of Herbal extract are commercially available in market. Become a medical use the potency of these extracts should be compatible & as per the standards prescribed in Pharmacopeia. Our aim is to evaluate the marketed extract sample and to check its authenticity and purity as per the standard parameter. The present study deals with preliminary phytochemical analysis & antibactertial activity of leaf with aqueous extract.

  19. Screening of Analgesic and Immunomodulator activity of Artocarpus heterophyllus Lam. Leaves (Jackfruit) in Mice

    OpenAIRE

    Jyoti; Om Prakash; Amit Kumar

    2013-01-01

    Adaptability is probably the most distinct characteristics of life which may be defined as sum of all nonspecific response of the body to any demands made upon it; fundamentally it was a physiological response; primary object of which was to maintain life and to re-establish the normal state. Analgesic and Immunomodulator activity of leaves of Artocarpus heterophyllus Lam. was evaluated by using Eddy’s hot plate method and Swimming endurance test at the dose levels of 250 and 500mg/kg in Swis...

  20. Screening of Vietnamese medicinal plants for NF-κB signaling inhibitors: Assessing the activity of flavonoids from the stem bark of Oroxylum indicum

    OpenAIRE

    Tran, Thi Van Anh; Malainer, Clemens; Schwaiger, Stefan; Hung, Tran; Atanasov, Atanas G.; Heiss, Elke H; Dirsch, Verena M.; Stuppner, Hermann

    2015-01-01

    Ethnopharmacological relevance Seventeen plants used in Vietnamese traditional medicine for the treatment of inflammatory disorders were screened for NF-κB inhibitory activity. Oroxylum indicum, which exhibited activity, was investigated in detail. Materials and methods Forty plant extracts from 17 species were prepared by maceration using dichloromethane and methanol and were tested (10 µg/mL) to evaluate their ability to inhibit NF-κB activation using TNF-α-stimulated HEK-293 cells stably t...