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Sample records for anti-infective activity screening

  1. Isolation, Phylogenetic Analysis and Anti-infective Activity Screening of Marine Sponge-Associated Actinomycetes

    Science.gov (United States)

    Abdelmohsen, Usama Ramadan; Pimentel-Elardo, Sheila M.; Hanora, Amro; Radwan, Mona; Abou-El-Ela, Soad H.; Ahmed, Safwat; Hentschel, Ute

    2010-01-01

    Terrestrial actinomycetes are noteworthy producers of a multitude of antibiotics, however the marine representatives are much less studied in this regard. In this study, 90 actinomycetes were isolated from 11 different species of marine sponges that had been collected from offshore Ras Mohamed (Egypt) and from Rovinj (Croatia). Phylogenetic characterization of the isolates based on 16S rRNA gene sequencing supported their assignment to 18 different actinomycete genera representing seven different suborders. Fourteen putatively novel species were identified based on sequence similarity values below 98.2% to other strains in the NCBI database. A putative new genus related to Rubrobacter was isolated on M1 agar that had been amended with sponge extract, thus highlighting the need for innovative cultivation protocols. Testing for anti-infective activities was performed against clinically relevant, Gram-positive (Enterococcus faecalis, Staphylococcus aureus) and Gram-negative (Escherichia coli, Pseudomonas aeruginosa) bacteria, fungi (Candida albicans) and human parasites (Leishmania major, Trypanosoma brucei). Bioactivities against these pathogens were documented for 10 actinomycete isolates. These results show a high diversity of actinomycetes associated with marine sponges as well as highlight their potential to produce anti-infective agents. PMID:20411105

  2. Marine Peptides and Their Anti-Infective Activities

    OpenAIRE

    Kang, Hee Kyoung; Seo, Chang Ho; Park, Yoonkyung

    2015-01-01

    Marine bioresources are a valuable source of bioactive compounds with industrial and nutraceutical potential. Numerous clinical trials evaluating novel chemotherapeutic agents derived from marine sources have revealed novel mechanisms of action. Recently, marine-derived bioactive peptides have attracted attention owing to their numerous beneficial effects. Moreover, several studies have reported that marine peptides exhibit various anti-infective activities, such as antimicrobial, antifungal,...

  3. Marine peptides and their anti-infective activities.

    Science.gov (United States)

    Kang, Hee Kyoung; Seo, Chang Ho; Park, Yoonkyung

    2015-01-16

    Marine bioresources are a valuable source of bioactive compounds with industrial and nutraceutical potential. Numerous clinical trials evaluating novel chemotherapeutic agents derived from marine sources have revealed novel mechanisms of action. Recently, marine-derived bioactive peptides have attracted attention owing to their numerous beneficial effects. Moreover, several studies have reported that marine peptides exhibit various anti-infective activities, such as antimicrobial, antifungal, antimalarial, antiprotozoal, anti-tuberculosis, and antiviral activities. In the last several decades, studies of marine plants, animals, and microbes have revealed tremendous number of structurally diverse and bioactive secondary metabolites. However, the treatments available for many infectious diseases caused by bacteria, fungi, and viruses are limited. Thus, the identification of novel antimicrobial peptides should be continued, and all possible strategies should be explored. In this review, we will present the structures and anti-infective activity of peptides isolated from marine sources (sponges, algae, bacteria, fungi and fish) from 2006 to the present.

  4. Marine Peptides and Their Anti-Infective Activities

    Directory of Open Access Journals (Sweden)

    Hee Kyoung Kang

    2015-01-01

    Full Text Available Marine bioresources are a valuable source of bioactive compounds with industrial and nutraceutical potential. Numerous clinical trials evaluating novel chemotherapeutic agents derived from marine sources have revealed novel mechanisms of action. Recently, marine-derived bioactive peptides have attracted attention owing to their numerous beneficial effects. Moreover, several studies have reported that marine peptides exhibit various anti-infective activities, such as antimicrobial, antifungal, antimalarial, antiprotozoal, anti-tuberculosis, and antiviral activities. In the last several decades, studies of marine plants, animals, and microbes have revealed tremendous number of structurally diverse and bioactive secondary metabolites. However, the treatments available for many infectious diseases caused by bacteria, fungi, and viruses are limited. Thus, the identification of novel antimicrobial peptides should be continued, and all possible strategies should be explored. In this review, we will present the structures and anti-infective activity of peptides isolated from marine sources (sponges, algae, bacteria, fungi and fish from 2006 to the present.

  5. 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.

  6. High-throughput screening for novel anti-infectives using a C. elegans pathogenesis model.

    Science.gov (United States)

    Conery, Annie L; Larkins-Ford, Jonah; Ausubel, Frederick M; Kirienko, Natalia V

    2014-03-14

    In recent history, the nematode Caenorhabditis elegans has provided a compelling platform for the discovery of novel antimicrobial drugs. In this protocol, we present an automated, high-throughput C. elegans pathogenesis assay, which can be used to screen for anti-infective compounds that prevent nematodes from dying due to Pseudomonas aeruginosa. New antibiotics identified from such screens would be promising candidates for treatment of human infections, and also can be used as probe compounds to identify novel targets in microbial pathogenesis or host immunity. Copyright © 2014 John Wiley & Sons, Inc.

  7. An anti-infective synthetic peptide with dual antimicrobial and immunomodulatory activities.

    Science.gov (United States)

    Silva, O N; de la Fuente-Núñez, C; Haney, E F; Fensterseifer, I C M; Ribeiro, S M; Porto, W F; Brown, P; Faria-Junior, C; Rezende, T M B; Moreno, S E; Lu, T K; Hancock, R E W; Franco, O L

    2016-11-02

    Antibiotic-resistant infections are predicted to kill 10 million people per year by 2050, costing the global economy $100 trillion. Therefore, there is an urgent need to develop alternative technologies. We have engineered a synthetic peptide called clavanin-MO, derived from a marine tunicate antimicrobial peptide, which exhibits potent antimicrobial and immunomodulatory properties both in vitro and in vivo. The peptide effectively killed a panel of representative bacterial strains, including multidrug-resistant hospital isolates. Antimicrobial activity of the peptide was demonstrated in animal models, reducing bacterial counts by six orders of magnitude, and contributing to infection clearance. In addition, clavanin-MO was capable of modulating innate immunity by stimulating leukocyte recruitment to the site of infection, and production of immune mediators GM-CSF, IFN-γ and MCP-1, while suppressing an excessive and potentially harmful inflammatory response by increasing synthesis of anti-inflammatory cytokines such as IL-10 and repressing the levels of pro-inflammatory cytokines IL-12 and TNF-α. Finally, treatment with the peptide protected mice against otherwise lethal infections caused by both Gram-negative and -positive drug-resistant strains. The peptide presented here directly kills bacteria and further helps resolve infections through its immune modulatory properties. Peptide anti-infective therapeutics with combined antimicrobial and immunomodulatory properties represent a new approach to treat antibiotic-resistant infections.

  8. Anti-infective activity of apolipoprotein domain derived peptides in vitro: identification of novel antimicrobial peptides related to apolipoprotein B with anti-HIV activity

    Directory of Open Access Journals (Sweden)

    McKnight Áine

    2010-03-01

    Full Text Available Abstract Background Previous reports have shown that peptides derived from the apolipoprotein E receptor binding region and the amphipathic α-helical domains of apolipoprotein AI have broad anti-infective activity and antiviral activity respectively. Lipoproteins and viruses share a similar cell biological niche, being of overlapping size and displaying similar interactions with mammalian cells and receptors, which may have led to other antiviral sequences arising within apolipoproteins, in addition to those previously reported. We therefore designed a series of peptides based around either apolipoprotein receptor binding regions, or amphipathic α-helical domains, and tested these for antiviral and antibacterial activity. Results Of the nineteen new peptides tested, seven showed some anti-infective activity, with two of these being derived from two apolipoproteins not previously used to derive anti-infective sequences. Apolipoprotein J (151-170 - based on a predicted amphipathic alpha-helical domain from apolipoprotein J - had measurable anti-HSV1 activity, as did apolipoprotein B (3359-3367 dp (apoBdp, the latter being derived from the LDL receptor binding domain B of apolipoprotein B. The more active peptide - apoBdp - showed similarity to the previously reported apoE derived anti-infective peptide, and further modification of the apoBdp sequence to align the charge distribution more closely to that of apoEdp or to introduce aromatic residues resulted in increased breadth and potency of activity. The most active peptide of this type showed similar potent anti-HIV activity, comparable to that we previously reported for the apoE derived peptide apoEdpL-W. Conclusions These data suggest that further antimicrobial peptides may be obtained using human apolipoprotein sequences, selecting regions with either amphipathic α-helical structure, or those linked to receptor-binding regions. The finding that an amphipathic α-helical region of

  9. Evaluation of Novel Antimicrobial Peptides as Topical Anti-Infectives with Broad-Spectrum Activity against Combat-Related Bacterial and Fungal Wound Infections

    Science.gov (United States)

    2017-10-01

    succeeded in developing resistance to a variety of AMPs. 2. Keywords Antimicrobial, peptides, anti-fungal, wounds, burns, bacterial resistance ...against Combat- Related Bacterial and Fungal Wound Infections PRINCIPAL INVESTIGATOR: Louis Edward Clemens Ph.D. CONTRACTING ORGANIZATION: Riptide...Anti-Infectives with Broad- Spectrum Activity against Combat-Related Bacterial and Fungal Wound Infections 5a. CONTRACT NUMBER 5b. GRANT NUMBER

  10. Antimicrobial activity of ceftaroline and other anti-infective agents against microbial pathogens recovered from the surgical intensive care patient population: a prevalence analysis.

    Science.gov (United States)

    Edmiston, Charles E; Krepel, Candace J; Leaper, David; Ledeboer, Nathan A; Mackey, Tami-Lea; Graham, Mary Beth; Lee, Cheong; Rossi, Peter J; Brown, Kellie R; Lewis, Brian D; Seabrook, Gary R

    2014-12-01

    Ceftaroline is a new parenteral cephalosporin agent with excellent activity against methicillin-sensitive (MSSA) and resistant strains of Staphylococcus aureus (MRSA). Critically ill surgical patients are susceptible to infection, often by multi-drug-resistant pathogens. The activity of ceftaroline against such pathogens has not been described. Three hundred thirty-five consecutive microbial isolates were collected from surgical wounds or abscesses, respiratory, urine, and blood cultures from patients in the surgical intensive care unit (SICU) of a major tertiary medical center. Using Clinical and Laboratory Standards Institute (CLSI) standard methodology and published breakpoints, all aerobic, facultative anaerobic isolates were tested against ceftaroline and selected comparative antimicrobial agents. All staphylococcal isolates were susceptible to ceftaroline at a breakpoint of ≤1.0 mcg/mL. In addition, ceftaroline exhibited excellent activity against all streptococcal clinical isolates and non-ESBL-producing strains of Enterobacteriaceae (93.5%) recovered from SICU patients. Ceftaroline was inactive against ESBL-producing Enterobacteriaceae, Pseudomonas aeruginosa, vancomycin-resistant enterococci, and selective gram-negative anaerobic bacteria. At present, ceftaroline is the only cephalosporin agent that is active against community and healthcare-associated MRSA. Further studies are needed to validate the benefit of this novel broad-spectrum anti-infective agent for the treatment of susceptible serious infections in the SICU patient population.

  11. 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

  12. Oligopeptide Targeting Sortase A as Potential Anti-infective Therapy for Staphylococcus aureus

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    Jianfeng Wang

    2018-02-01

    Full Text Available Sortase A (SrtA-catalyzed anchorage of surface proteins in most Gram-positive bacteria is indispensable for their virulence, suggesting that this transpeptidase is a promising target for antivirulence therapy. Here, an oligopeptide, LPRDA, was identified as an effective inhibitor of SrtA via virtual screening based on the LPXTG substrate sequence, and it was found to inhibit SrtA activity in vitro and in vivo (IC50 = 10.61 μM by competitively occupying the active site of SrtA. Further, the oligopeptide treatment had no anti-Staphylococcus aureus activity, but it provided protection against S. aureus-induced mastitis in a mouse model. These findings indicate that the oligopeptide could be used as an effective anti-infective agent for the treatment of infection caused by S. aureus or other Gram-positive bacteria via the targeting of SrtA.

  13. Bioprospecting Micromonospora from Kaziranga National Park of India and their anti-infective potential.

    Science.gov (United States)

    Talukdar, Madhumita; Duarah, Aparajita; Talukdar, Shruti; Gohain, Manorama Bura; Debnath, Rajal; Yadav, Archana; Jha, Dhruva K; Bora, Tarun C

    2012-08-01

    Large number of strains was isolated from soils of Kaziranga National Park of North-East India using selective isolation procedure. They were assigned to the genus Micromonospora on the basis of their typical colonial and pigmentation features. The taxonomic identities of the isolates were confirmed on the basis of their molecular characters (16SrDNA). A total of one hundred Micromonospora strains were isolated during the present investigation. The diagnostic cell wall sugar and amino acids were determined from these Micromonospora strains. After preliminary screening most of the isolates exhibited excellent anti-infective activity against human bacterial pathogens Staphylococcus aureas, Bacillus subtilis, Proteus vulgaris, Echerichia coli, Pseudomonas aeroginosa and fungal pathogens Aspergillus niger, Fusarium oxysporum and Candida albicans. Among these isolates one strain designated as HK-10 showed promising activity against human pathogens S. aureas, B. subtilis, P. vulgaris and P. aeroginosa.

  14. 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...

  15. Evaluation of Novel Antimicrobial Peptides as Topical Anti-Infectives with Broad Spectrum Activity Against Combat-Related Bacterial and Fungal Wound Infections

    Science.gov (United States)

    2016-10-01

    absence of topical antibiotics, are immediately colonized by gram-positive skin flora, such as Staphylococcus aureus. Gram-negative bacteria such as...in a wound, as the dAMP is metabolized and/or diluted with tissue fluids, it will continue to be active. We are aware that the peptides will be

  16. 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

    2014-01-01

    SUMMARY 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. PMID:24696432

  17. 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.

  18. Anti-infective and wound healing properties of Flabellaria paniculata ...

    African Journals Online (AJOL)

    Anti-infective and wound healing properties of Flabellaria paniculata. A Abo, JAO Olugbuyiro, SA Famakinde ... was recorded in Pseudomonas aeruginosa group on day 18. This drug is anti-infective as well as wound healing agent thus justifying the local uses of the plant for the treatment of skin diseases and sores.

  19. phytochemical screening, antibacterial and toxicological activities

    African Journals Online (AJOL)

    Dealer

    The phytochemical screening, antibacterial and toxicological activities of extracts of the stem bark of Acacia senegal were investigated. ... Keywords: Phytochemical Screening, Antibacterial Activity, Toxicological Activity Acacia senegal,. Extracts. INTRODUCTION ..... Vegetable Drugs; Chemical Industries. Branch; Division of ...

  20. Chalcone scaffolds as anti-infective agents: structural and molecular target perspectives.

    Science.gov (United States)

    Mahapatra, Debarshi Kar; Bharti, Sanjay Kumar; Asati, Vivek

    2015-08-28

    In recent years, widespread outbreak of numerous infectious diseases across the globe has created havoc among the population. Particularly, the inhabitants of tropical and sub-tropical regions are mainly affected by these pathogens. Several natural and (semi) synthetic chalcones deserve the credit of being potential anti-infective candidates that inhibit various parasitic, malarial, bacterial, viral, and fungal targets like cruzain-1/2, trypanopain-Tb, trans-sialidase, glyceraldehyde-3-phosphate dehydrogenase (GAPDH), fumarate reductase, falcipain-1/2, β-hematin, topoisomerase-II, plasmepsin-II, lactate dehydrogenase, protein kinases (Pfmrk and PfPK5), and sorbitol-induced hemolysis, DEN-1 NS3, H1N1, HIV (Integrase/Protease), protein tyrosine phosphatase A/B (Ptp-A/B), FtsZ, FAS-II, lactate/isocitrate dehydrogenase, NorA efflux pump, DNA gyrase, fatty acid synthase, chitin synthase, and β-(1,3)-glucan synthase. In this review, a comprehensive study (from Jan. 1982 to May 2015) of the structural features of anti-infective chalcones, their mechanism of actions (MOAs) and structure activity relationships (SARs) have been highlighted. With the knowledge of molecular targets, structural insights and SARs, this review may be helpful for (medicinal) chemists to design more potent, safe, selective and cost effective anti-infective agents. Copyright © 2015 Elsevier Masson SAS. All rights reserved.

  1. 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.

  2. Phytochemical Screening, Antibacterial and Toxicological Activities ...

    African Journals Online (AJOL)

    The phytochemical screening, antibacterial and toxicological activities of extracts of the stem bark of Acacia senegal were investigated. The phytochemical analyses according to standard screening tests using conventional protocols revealed the presence of tannins, saponins and sterols in the stem bark of the plant.

  3. Phytochemical screening and antibacterial activity of Cissampelos ...

    African Journals Online (AJOL)

    Phytochemical screening and antibacterial activity of Cissampelos mucronata a. Rich (Menispermaceae) extracts. T A Tor-Anyiin, R Sha'ato, H O Oluma. Abstract. Phytochemical screening of various extracts of Cissampelos mucronata, obtained using soxhlet apparatus showed presence of alkaloids, tannins and saponins.

  4. Phytochemical Screening and Antibacterial Activities Of HIBISCUS ...

    African Journals Online (AJOL)

    USER

    46. Nigerian Journal of Chemical Research. Vol. 20, 2015. Phytochemical Screening and Antibacterial Activities Of HIBISCUS SABDARIFFA L. Leaf Extracts. Adamu, H. ... extract of the leaves of Hibiscus sabdariffa L. The mean zones of inhibition of the methanolic leaf extracts ... drink is popularly known as zobo in Nigeria.

  5. Preliminary Phytochemical Screening and Antimicrobial Activities of ...

    African Journals Online (AJOL)

    Dried leaves of Abrus precatorius, Desmodium ramosissimum, Scoparia dulcis and aerial parts of Phyllanthus amarus used in folkloric medicine of Ebiraland were extracted with hexane, methanol and water sequentially using soxhlet apparatus. The extracts were screened for antimicrobial activities against Bacillus subtilis, ...

  6. Light based anti-infectives: ultraviolet C irradiation, photodynamic therapy, blue light, and beyond

    Science.gov (United States)

    Yin, Rui; Dai, Tianhong; Avci, Pinar; Jorge, Ana Elisa Serafim; de Melo, Wanessa CMA; Vecchio, Daniela; Huang, Ying-Ying; Gupta, Asheesh; Hamblin, Michael R

    2013-01-01

    Owing to the worldwide increase in antibiotic resistance, researchers are investigating alternative anti-infective strategies to which it is supposed microorganisms will be unable to develop resistance. Prominent among these strategies, is a group of approaches which rely on light to deliver the killing blow. As is well known, ultraviolet light, particularly UVC (200–280nm), is germicidal, but it has not been much developed as an anti-infective approach until recently, when it was realized that the possible adverse effects to host tissue were relatively minor compared to its high activity in killing pathogens. Photodynamic therapy is the combination of non-toxic photosensitizing dyes with harmless visible light that together produce abundant destructive reactive oxygen species (ROS). Certain cationic dyes or photosensitizers have good specificity for binding to microbial cells while sparing host mammalian cells and can be used for treating many localized infections, both superficial and even deep-seated by using fiber optic delivered light. Many microbial cells are highly sensitive to killing by blue light (400–470 nm) due to accumulation of naturally occurring photosensitizers such as porphyrins and flavins. Near infrared light has also been shown to have antimicrobial effects against certain species. Clinical applications of these technologies include skin, dental, wound, stomach, nasal, toenail and other infections which are amenable to effective light delivery. PMID:24060701

  7. Light based anti-infectives: ultraviolet C irradiation, photodynamic therapy, blue light, and beyond.

    Science.gov (United States)

    Yin, Rui; Dai, Tianhong; Avci, Pinar; Jorge, Ana Elisa Serafim; de Melo, Wanessa C M A; Vecchio, Daniela; Huang, Ying-Ying; Gupta, Asheesh; Hamblin, Michael R

    2013-10-01

    Owing to the worldwide increase in antibiotic resistance, researchers are investigating alternative anti-infective strategies to which it is supposed microorganisms will be unable to develop resistance. Prominent among these strategies, is a group of approaches which rely on light to deliver the killing blow. As is well known, ultraviolet light, particularly UVC (200-280 nm), is germicidal, but it has not been much developed as an anti-infective approach until recently, when it was realized that the possible adverse effects to host tissue were relatively minor compared to its high activity in killing pathogens. Photodynamic therapy is the combination of non-toxic photosensitizing dyes with harmless visible light that together produce abundant destructive reactive oxygen species (ROS). Certain cationic dyes or photosensitizers have good specificity for binding to microbial cells while sparing host mammalian cells and can be used for treating many localized infections, both superficial and even deep-seated by using fiber optic delivered light. Many microbial cells are highly sensitive to killing by blue light (400-470 nm) due to accumulation of naturally occurring photosensitizers such as porphyrins and flavins. Near infrared light has also been shown to have antimicrobial effects against certain species. Clinical applications of these technologies include skin, dental, wound, stomach, nasal, toenail and other infections which are amenable to effective light delivery. Copyright © 2013 Elsevier Ltd. All rights reserved.

  8. Biological activity screening of seven Plectranthus species

    OpenAIRE

    Epole Ntungwe N; Joana Marçalo; Catarina Garcia; Catarina Reis; Catarina Teodósio; Carolina Oliveira; Cláudia Oliveira; Amílcar Roberto; Patrícia Rijo

    2017-01-01

    Natural products from Plectranthus spp. plants have an ethnopharmacological use, inspiring several scientific investigations. As such, this work aims to perform a biological activity screening in order to scientifically validate the use of these plants. Assays on in vitro acetylcholinesterase (AChE) inhibition, antioxidant effects, antimicrobial activity and Artemia salina lethality were performed on seven Plectranthus spp. extracts (P. swynnertonii, P. welwischii, P. woodii, P. cylindraceus,...

  9. Innovative Approaches to Improve Anti-Infective Vaccine Efficacy.

    Science.gov (United States)

    Yeaman, Michael R; Hennessey, John P

    2017-01-06

    Safe and efficacious vaccines are arguably the most successful medical interventions of all time. Yet the ongoing discovery of new pathogens, along with emergence of antibiotic-resistant pathogens and a burgeoning population at risk of such infections, imposes unprecedented public health challenges. To meet these challenges, innovative strategies to discover and develop new or improved anti-infective vaccines are necessary. These approaches must intersect the most meaningful insights into protective immunity and advanced technologies with capabilities to deliver immunogens for optimal immune protection. This goal is considered through several recent advances in host-pathogen relationships, conceptual strides in vaccinology, and emerging technologies. Given a clear and growing risk of pandemic disease should the threat of infection go unmet, developing vaccines that optimize protective immunity against high-priority and antibiotic-resistant pathogens represents an urgent and unifying imperative.

  10. Biological activity screening of seven Plectranthus species

    Directory of Open Access Journals (Sweden)

    Epole Ntungwe N

    2017-07-01

    Full Text Available Natural products from Plectranthus spp. plants have an ethnopharmacological use, inspiring several scientific investigations. As such, this work aims to perform a biological activity screening in order to scientifically validate the use of these plants. Assays on in vitro acetylcholinesterase (AChE inhibition, antioxidant effects, antimicrobial activity and Artemia salina lethality were performed on seven Plectranthus spp. extracts (P. swynnertonii, P. welwischii, P. woodii, P. cylindraceus, P. spicatus, P. ramosior and P. petiolaris. Acetonic extracts were obtained by sonication (10% w/v, where P. ramosior had the highest yield of dry extract (13.49% w/w. In the AChE inhibition assay, only P. cylindraceus extract decreased enzymatic activity (30.2 ± 3.78%. The antimicrobial activity was screened using the well diffusion method, against Gram positive and negative bacteria and yeast. P. ramosior extract showed not only an inhibition zone against S. aureus and C. albicans (15 and 11 mm, respectively, but also the highest scavenging activity (DPPH method, 36.4 ± 0.04%. On the lethality test in A. salina, P. swynnertonnii extract was the most toxic (LC50 = 0.036 mg/L. These preliminary results showed that P. cylindraceus, P. ramosior and P. swynnertonnii are potential bioactive extracts for further isolation and antimicrobial and cytotoxic studies.

  11. Gender differences in the use of anti-infective medications before and after widowhood

    DEFF Research Database (Denmark)

    Santacroce, Adriana; Wastesson, Jonas W; Höhn, Andreas

    2018-01-01

    widowhood among both men and women. Also, age-related changes in the use of anti-infective medications were similar in both genders. CONCLUSIONS: The present study shows that individuals are more likely to use anti-infective medication after being widowed than before being widowed, but this change is likely...... to be related to increasing age and it is similar in both genders....

  12. γδ-T cells: an unpolished sword in human anti-infection immunity.

    Science.gov (United States)

    Zheng, Jian; Liu, Yinping; Lau, Yu-Lung; Tu, Wenwei

    2013-01-01

    γδ-T cells represent a small population of immune cells, but play an indispensable role in host defenses against exogenous pathogens, immune surveillance of endogenous pathogenesis and even homeostasis of the immune system. Activation and expansion of γδ-T cells are generally observed in diverse human infectious diseases and correlate with their progression and prognosis. γδ-T cells have both 'innate' and 'adaptive' characteristics in the immune response, and their anti-infection activities are mediated by multiple pathways that are under elaborate regulation by other immune components. In this review, we summarize the current state of the literature and the recent advancements in γδ-T cell-mediated immune responses against common human infectious pathogens. Although further investigation is needed to improve our understanding of the characteristics of different γδ-T cell subpopulations under specific conditions, γδ-T cell-based therapy has great potential for the treatment of infectious diseases.

  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. Anti-Infective Potential of Marine Invertebrates and Seaweeds from the Brazilian Coast

    Directory of Open Access Journals (Sweden)

    Mario Steindel

    2013-05-01

    Full Text Available This manuscript describes the evaluation of anti-infective potential in vitro of organic extracts from nine sponges, one ascidian, two octocorals, one bryozoan, and 27 seaweed species collected along the Brazilian coast. Antimicrobial activity was tested against Staphylococcus aureus (ATCC 25923, Enterococcus faecalis (ATCC 29212, Pseudomonas aeruginosa (ATCC 27853, Escherichia coli (ATCC 25922 and Candida albicans (ATCC 10231 by the disk diffusion method. Antiprotozoal activity was evaluated against Leishmania braziliensis (MHOM/BR/96/LSC96-H3 promastigotes and Trypanosoma cruzi (MHOM/BR/00/Y epimastigotes by MTT assay. Activity against intracellular amastigotes of T. cruzi and L. brasiliensis in murine macrophages was also evaluated. Antiviral activity was tested against Herpes Simplex Virus type 1 (HSV-1, KOS strain by the plaque number reduction assay (IC50. Cytotoxicity on VERO cells was evaluated by the MTT assay (CC50. The results were expressed as SI = CC50/IC50. The most promising antimicrobial results were obtained against S. aureus and C. albicans with Dragmacidon reticulatum. Among the seaweeds, only Osmundaria obtusiloba showed moderate activity against P. aeruginosa. Concerning antiprotozoal activity, Bugula neritina, Carijoa riseii, Dragmaxia anomala and Haliclona (Halichoclona sp. showed the most interesting results, mainly against extracellular promastigote forms of L. braziliensis (66, 35.9, 97.2, and 43.6% inhibition, respectively. Moreover, six species of seaweeds Anadyomene saldanhae, Caulerpa cupressoides, Canistrocarpus cervicornis, Dictyota sp., Ochtodes secundiramea, and Padina sp. showed promising results against L. braziliensis (87.9, 51.7, 85.9, 93.3, 99.7, and 80.9% inhibition, respectively, and only Dictyota sp. was effective against T. cruzi (60.4% inhibition. Finally, the antiherpes activity was also evaluated, with Haliclona (Halichoclona sp. and Petromica citrina showing the best results (SI = 11.9 and SI > 5

  15. Physical Activity and Screen Time in Adolescents and Their Friends

    Science.gov (United States)

    Sirard, John R.; Bruening, Meg; Wall, Melanie M.; Eisenberg, Marla E.; Kim, Sun K.; Neumark-Sztainer, Dianne

    2012-01-01

    Background Little is known about the actual physical activity and screen time behaviors of an adolescent’s friends relative to the individual’s behavior. Purpose To determine the associations between an adolescent’s physical activity and screen time and his/her nominated friends’ physical activity and screen time. Methods Data were obtained from EAT 2010 (Eating and Activity Among Teens), a large cross-sectional study (n=2126) conducted in 20 middle schools and high schools in Minneapolis/St. Paul MN during the 2009–2010 academic year and analyzed during 2011. Each participant nominated up to six friends from a school roster, and data from those friends were obtained as part of the school-based data collection procedures. Physical activity and screen time were assessed with previously used and validated questionnaires. Generalized estimating equation models, stratified by gender, were used to assess associations between adolescents’ physical activity and screen time and their friends’ physical activity and screen time. Results Physical activity for female adolescents was associated with their male and female friends’ physical activity, including their male and female best friends (all pphysical activity was associated with their female friends’ physical activity (padolescents’ physical activity and their friends’ physical activity indicates a need to include peer effects on adolescent female physical activity in future intervention work. PMID:23253649

  16. Biocompatible Silver Nanoparticle-Modified Natural Diatomite with Anti-Infective Property

    Directory of Open Access Journals (Sweden)

    Haolin Sun

    2018-01-01

    Full Text Available Nanosilver as an alternative antibacterial agent of antibiotics has been researched for possible applications in various orthopedic implants. However, it is imperative to achieve controllable release of Ag+ to reduce its cytotoxic effect on normal tissue. Here, a nanosilver release system that has potential to be used in anti-infective bone cement was reported. Nanosilver modified diatomite was developed through the reaction of Tollens’ reagent to improve the antibacterial effect and natural diatomite was used as the carrier of Ag+ ions for controlled release. Cytotoxicity and the antibacterial activities of the nanosilver release system were characterized. After 3 days, the NIH3T3 cells cultured in the extract of nanosilver modified diatomite with an initial concentration of 0.5 mg/ml showed better cell viability than cells cultured in α-MEM. The density of MC3T3-E1 cells cultured in the extract of nanosilver modified diatomite at the same concentration did not differ significantly from the density of cells cultured in α-MEM. The nanosilver modified diatomite exhibited antibacterial effect against E. coli and S. aureus when the concentration was higher than 0.5 mg/ml. With appropriate selection of Ag+ concentration, the nanosilver modified diatomite is promising for improving the antibacterial effect while not affecting the biocompatibility of reinforced calcium phosphate bone cement.

  17. Infections and exposure to anti-infective agents and the risk of severe mental disorders

    DEFF Research Database (Denmark)

    Köhler, Ole; Petersen, Liselotte; Mors, O

    2017-01-01

    OBJECTIVE: Severe infections are associated with increased risks of mental disorders; however, this is the first large-scale study investigating whether infections treated with anti-infective agents in the primary care setting increase the risks of schizophrenia and affective disorders. METHOD: W....../inflammation on the brain, alterations of the microbiome, genetics, or other environmental factors.......OBJECTIVE: Severe infections are associated with increased risks of mental disorders; however, this is the first large-scale study investigating whether infections treated with anti-infective agents in the primary care setting increase the risks of schizophrenia and affective disorders. METHOD: We...... identified all individuals born in Denmark 1985-2002 (N = 1 015 447) and studied the association between infections treated with anti-infective agents and the subsequent risk of schizophrenia and affective disorders during 1995-2013. Cox regression analyses were adjusted for important confounders. RESULTS...

  18. Phytochemical screening for antibacterial activity of potential ...

    African Journals Online (AJOL)

    Plants have been identified for their valuable properties for traditional medicine since thousands of years ago. The huge diversity of the Malaysian flora that has chemical diversity is one of the vital factors that make natural products outstanding candidates for any screening practice. In this study, the leaves of five local plants ...

  19. Antimicrobial Activity and Phytochemical Screening of Ficus ...

    African Journals Online (AJOL)

    Prelimlinary phytochemical screening of Ficus exasperata root bark showed that it contains saponin, alkaloids, cardiac glycoside and reducing sugar with no traces of tannin and anthraquinone. The results of the study provide scientific basis for developing a novel broad spectrum antimicrobial herbal formulation in future.

  20. 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.

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

    Science.gov (United States)

    Serrano-Sanchez, Jose A; Martí-Trujillo, Sara; Lera-Navarro, Angela; Dorado-García, Cecilia; González-Henríquez, Juan J; Sanchís-Moysi, Joaquín

    2011-01-01

    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. 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. 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.

  2. 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 beverag...

  3. Global occurrence of anti-infectives in contaminated surface waters: Impact of income inequality between countries.

    Science.gov (United States)

    Segura, Pedro A; Takada, Hideshige; Correa, José A; El Saadi, Karim; Koike, Tatsuya; Onwona-Agyeman, Siaw; Ofosu-Anim, John; Sabi, Edward Benjamin; Wasonga, Oliver V; Mghalu, Joseph M; dos Santos Junior, Antonio Manuel; Newman, Brent; Weerts, Steven; Yargeau, Viviane

    2015-07-01

    The presence anti-infectives in environmental waters is of interest because of their potential role in the dissemination of anti-infective resistance in bacteria and other harmful effects on non-target species such as algae and shellfish. Since no information on global trends regarding the contamination caused by these bioactive substances is yet available, we decided to investigate the impact of income inequality between countries on the occurrence of anti-infectives in surface waters. In order to perform such study, we gathered concentration values reported in the peer-reviewed literature between 1998 and 2014 and built a database. To fill the gap of knowledge on occurrence of anti-infectives in African countries, we also collected 61 surface water samples from Ghana, Kenya, Mozambique and South Africa, and measured concentrations of 19 anti-infectives. A mixed one-way analysis of covariance (ANCOVA) model, followed by Turkey-Kramer post hoc tests was used to identify potential differences in anti-infective occurrence between countries grouped by income level (high, upper-middle and lower-middle and low income) according to the classification by the World Bank. Comparison of occurrence of anti-infectives according to income level revealed that concentrations of these substances in contaminated surface waters were significantly higher in low and lower-middle income countries (p=0.0001) but not in upper-middle income countries (p=0.0515) compared to high-income countries. We explained these results as the consequence of the absence of or limited sewage treatment performed in lower income countries. Furthermore, comparison of concentrations of low cost anti-infectives (sulfonamides and trimethoprim) and the more expensive macrolides between income groups suggest that the cost of these substances may have an impact on their environmental occurrence in lower income countries. Since wastewaters are the most important source of contamination of anti-infectives and other

  4. 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.

  5. 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

  6. Besifloxacin: a novel anti-infective for the treatment of bacterial conjunctivitis

    Directory of Open Access Journals (Sweden)

    Timothy L Comstock

    2010-03-01

    Full Text Available Timothy L Comstock1, Paul M Karpecki2, Timothy W Morris3, Jin-Zhong Zhang41Global Medical Affairs, Pharmaceuticals, Bausch and Lomb, Inc., Rochester, NY, USA; 2Koffler Vision Group, Lexington, KY, USA; 3Research and Development Microbiology and Sterilization Sciences, Bausch and Lomb, Inc., Rochester, NY, USA; 4Global Preclinical Development, Bausch and Lomb, Inc., Rochester, NY, USAAbstract: Bacterial conjunctivitis, commonly known as pink eye, is demographically unbiased in its prevalence and can be caused by a variety of aerobic and anaerobic bacteria. Timely empiric treatment with a broad-spectrum anti-infective, such as a topical fluoroquinolone, is critical in preventing potentially irreversible ocular damage. However, the rise in ocular methicillin-resistant Staphylococcus aureus isolates and the patterns of fluoroquinolone resistance for patients with other ocular bacterial infections mandate the need for new agents targeted for ocular use. Besifloxacin, a novel broad-spectrum fluoroquinolone, is approved for the treatment of bacterial conjunctivitis. It has a uniquely balanced dual-targeting activity that inhibits both DNA gyrase and topoisomerase IV and is associated with a lower incidence of resistance development. Besifloxacin is not marketed in other formulations, ensuring that its exposure is limited to bacterial populations in and around the eye. This specifically precludes any bacterial exposure to besifloxacin resulting from systemic use, which further reduces the likelihood of emergence of bacterial resistance. In vitro, besifloxacin has demonstrated equivalent or superior activity compared with other commonly used topical antibiotics. In clinical trials, besifloxacin has consistently demonstrated efficacy and safety in the treatment of patients with bacterial conjunctivitis. Besifloxacin is considered safe and is well tolerated with no observed contraindications.Keywords: conjunctivitis, fluoroquinolones, besifloxacin

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

    OpenAIRE

    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-...

  8. Screen Fingerprints as a Novel Modality for Active Authentication

    Science.gov (United States)

    2014-03-01

    biometrics such as face and iris recognition has become more reliable. Yet, its dependence on hardware sensors often limits its applicability. On the...as a new biometric modality for active authentication. Such a fingerprint is acquired by taking a screen recording of the computer being used and...extracting discriminative visual feature from the recording. 15. SUBJECT TERMS Active authentication, screen fingerprints, biometrics 16. SECURITY

  9. An Independent Evaluation of a Novel Peptide Mimetic, Brilacidin (PMX30063), for Ocular Anti-Infective

    Science.gov (United States)

    Romanowski, Eric G.; Yates, Kathleen A.; Mah, Francis S.

    2016-01-01

    Abstract Purpose: Brilacidin (BRI), a novel defensin mimetic, was evaluated as an ocular anti-infective. Methods: In vitro: Potency based on MIC90s was compared for 50 Staphylococcus aureus (SA), 50 Staphylococcus epidermidis (SE), and 25 each of Streptococcus pneumonia (SP), Streptococcus viridans (SV), Moraxella (MS), Haemophilus influenzae (HI), Pseudomonas aeruginosa (PA), and Serratia marcescens (SM). In vivo: Using established methods, ocular toxicity was graded with Draize testing. For efficacy testing, both corneas of 24 rabbits were infected with methicillin-resistant S. aureus (MRSA), whereas the corneal epithelium was removed in the left eye. After 4 h, 21 topical drops over 5 h were administered to 4 groups: BRI 0.5%, vancomycin (VAN) 5%, saline, and no treatment. The eyes were clinically graded and the corneas were harvested for colony counts. Results: In vitro: Both SA and SE had the lowest minimum inhibitory concentrations among the bacterial groups. The MIC90s to BRI for SP, SV, MS, HI, PA, and SM were 4, 32, 256, 32, 16, and 128-fold higher, respectively, than SA and SE. In vivo: Draize testing determined BRI 0.5% to be minimally irritating. For abraded corneas, BRI was not statistically different from VAN for reducing MRSA. BRI was bactericidal. For intact corneas, VAN reduced more CFU than BRI. BRI reduced CFU in abraded corneas more than intact corneas suggesting poor corneal penetration. Conclusions: BRI has Gram-positive in vitro activity; topical BRI 0.5% was minimally irritating; and BRI 0.5% was equally efficacious as VAN in a MRSA keratitis model when the corneal epithelium was removed. PMID:26501484

  10. Ultrashort self-assembling Fmoc-peptide gelators for anti-infective biomaterial applications.

    Science.gov (United States)

    McCloskey, Alice P; Draper, Emily R; Gilmore, Brendan F; Laverty, Garry

    2017-02-01

    Biomaterial-related infections have a significant impact on society and are a major contributor to the growing threat of antimicrobial resistance. Current licensed antibiotic classes struggle to breakdown or penetrate the exopolysaccharide biofilm barrier, resulting in sub-therapeutic concentrations of antibiotic at the surface of the biomaterial, treatment failure and increased spread of resistant isolates. This paper focuses for the first time on the ability of ultrashort Fmoc-peptide gelators to eradicate established bacterial biofilms implicated in a variety of medical device infections (Gram-positive: Staphylococcus aureus, Staphylococcus epidermidis and Gram-negative Escherichia coli, Pseudomonas aeruginosa). The effect of increasing the cationicity of FmocFF via addition of di-lysine and di-orntithine was also studied with regard to antibacterial activity. Our studies demonstrated that Fmoc-peptides (FmocFF, FmocFFKK, FmocFFFKK, FmocFFOO) formed surfactant-like soft gels at concentrations of 1% w/v and above using a method of glucono-δ-Lactone pH induction. The majority of Fmoc-peptides (0.5-2% w/v) demonstrated selective action against established (grown for 24 h) biofilms of Gram-positive and Gram-negative pathogens. These results are likely to increase the clinical translation of short-peptide gelator platforms within the area of anti-infective biomaterials including as wound dressings and coatings for prostheses, catheters, heart valves and surgical tubes. In the long term, this will lead to wider treatment choices for clinicians and patients involved in the management of medical device infections and reduce the burden of antimicrobial resistance. Copyright © 2017 European Peptide Society and John Wiley & Sons, Ltd. Copyright © 2017 European Peptide Society and John Wiley & Sons, Ltd.

  11. Preliminary phytochemical screening and antioxidant activity of ...

    African Journals Online (AJOL)

    GAE) and the reducing power of 0.071±0.03nm was obtained. The DPPH scavenging activity of the extract was found to be promising. There is no significant difference (p<0.05) in the antioxidant activity between the extract and those of the ...

  12. Preliminary phytochemical screening and antimicrobial activity of ...

    African Journals Online (AJOL)

    The methanol, ethyl acetate and chloroform extracts demonstrated promising activity against the test organisms. The activity of methanol extract was more pronounced against C. albicans (42mm) while that of petroleum ether extract was the least against E.coli (6mm). However, S. typhi and E. coli were resistant to chloroform ...

  13. Phytochemical Screening, Antibacterial and Toxicological Activities ...

    African Journals Online (AJOL)

    The extract fractions generally exhibited marked antibacterial activities on Klebsiella pneumoniae, Pseudomonas aeruginosa, Proteus vulgaris, Salmonella typhi, Shigella dysenteriae Staphylococcus aureus and Escherichia coli except on Streptococcus pneumoniae and Streptococcus pyogenes. All the leaves extract ...

  14. ACTIVE PRODUCERS OF PEROXIDASE BASIDIOMYCETES STRAINS SCREENING

    Directory of Open Access Journals (Sweden)

    T. E. Voloshko

    2013-10-01

    Full Text Available The paper is devoted to the analysis of the research data peroxidase activity of the strains of xylotrophic basidiomycetes in the dynamics of the growth. The objects of study were 57 strains, 5 of which belongs to 5 species of the order Polyporales, and 52 of which belongs to 7 species of the order Agaricales. In order to search for active producers of peroxidase the strains were cultured by the surface method in a liquid glucosepeptone medium. The accumulation of oven-dry biomass was determined by the weight method. The content of soluble protein and peroxidase activity were determined by the spectrophotometry. The studies set the level of accumulation of oven-dry biomass and peroxidase activity of the strains in 9 and 12 days of growth. The results allowed selecting the strains, which are characterized by high levels of peroxidase activity in mycelium and in the culture filtrate, including Agrocybe cylindracea 167, Pleurotus ostreatus Р-кл, Agrocybe cylindracea 960 and 218. These strains which are active producers of peroxidase may be used in the enzyme preparations obtaining technology.

  15. Screening of natural extracts for their antibacterial activity against ...

    African Journals Online (AJOL)

    Screening of natural extracts for their antibacterial activity against different enteric pathogens isolated from soil, water and rotten fruit samples. ... The antibacterial activity of crude extract was comparable with ciprofloxacin and ceftriaxone, commonly used antibiotics for the treatment of infections in adults and children, ...

  16. Novel Anti-Infective Compounds from Marine Bacteria

    Directory of Open Access Journals (Sweden)

    Hafizur Rahman

    2010-03-01

    Full Text Available As a result of the continuous evolution of microbial pathogens towards antibiotic-resistance, there have been demands for the development of new and effective antimicrobial compounds. Since the 1960s, the scientific literature has accumulated many publications about novel pharmaceutical compounds produced by a diverse range of marine bacteria. Indeed, marine micro-organisms continue to be a productive and successful focus for natural products research, with many newly isolated compounds possessing potentially valuable pharmacological activities. In this regard, the marine environment will undoubtedly prove to be an increasingly important source of novel antimicrobial metabolites, and selective or targeted approaches are already enabling the recovery of a significant number of antibiotic-producing micro-organisms. The aim of this review is to consider advances made in the discovery of new secondary metabolites derived from marine bacteria, and in particular those effective against the so called “superbugs”, including methicillin-resistant Staphylococcus aureus (MRSA and vancomycin resistant enterococci (VRE, which are largely responsible for the increase in numbers of hospital acquired, i.e., nosocomial, infections.

  17. preliminary phytochemical screening and antioxidant activity

    African Journals Online (AJOL)

    DR. AMINU

    ABSTRACT. Antioxidant evaluation of Albizia chevalieri used in Northern Nigerian traditional medicine, was carried out using the free radical scavenging activity of the 1, 1-diphenyl-2-picrylhydrazyl radical. (DPPH), total phenolics content and reducing power assay on the methanol leave extract. The results of the DPPH ...

  18. Phytochemical Screening and Antioxidant Activities of Some ...

    African Journals Online (AJOL)

    Purpose: Oxidative stress has been shown to play an important role in the development of anaemia in malaria. Indeed, increase in total antioxidant status has been shown to be important in recovery from malaria. The antioxidant activities of four medicinal plants traditionally used in the treatment of malaria in southwestern ...

  19. Phytochemical screening and antibacterial activity of Azadiracta ...

    African Journals Online (AJOL)

    Preliminary phytochemical analysis showed that both stem bark and leaf extracts contain alkaloid, tannin, anthraquinone, flavonoid, phenols and terpenoid. The extracts of the plant demonstrated antibacterial activity due to presence of phytochemical constituents hence, the application of the decoction of leaf and stem bark ...

  20. Phytochemical Screening and Antibacterial Activity of Cybopogon ...

    African Journals Online (AJOL)

    Similarly, the results of antibacterial activity testing of the extracts at equal disc concentration of 30@g/disc showed that E. coli was sensitive to all extracts with inhibition zone diameters of 7mm, Klebsiella spp. and Proteus spp. were sensitive to acetone extract of the plant with inhibition zone diameters of 7mm each while ...

  1. [Cervical cancer screening: Is active recruitment worth the effort?].

    Science.gov (United States)

    Morales Martínez, Ángeles; Blanco Rodríguez, Lorena; Morales Martínez, Cristina; Tejuca Somoano, Sonia

    2015-12-01

    To determine the percentage of women who have had a Pap smear in the last 5 years, and the place where it was carried out. To detect cytological abnormalities and precursors of cervical cancer in un-screened or inadequately screened women and the prevalence of HPV-positive determinations. Cross sectional study. Natahoyo Health Centre, Gijón (Spain). Women aged 40-50 years living in the area and assigned to the Health Centre. The information was collected from databases, telephone and home surveys. There was active recruitment of unscreened women or inadequately screened in Primary Care as well as offering to perform cytology and HPV determination. Of the 1420 women aged 40 to 50 years, 1236 (87%) had cytology in the last 5 years, and 184 women (13%) had no screening or it was inadequate. Of these 184 women, 108 (58.7%) agreed to have cytology and HPV test performed. No high-grade cervical dysplasia was diagnosed. The prevalence of HPV-positive was 8.3%. In our population there is a high coverage of opportunistic screening for cervical cancer. The active recruitment of women who were not in the screening program was not useful. Copyright © 2014 Elsevier España, S.L.U. All rights reserved.

  2. 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. Copyright © 2014. Published by Elsevier SAS.

  3. A review of the clinical implications of anti-infective biomaterials and infection-resistant surfaces.

    Science.gov (United States)

    Campoccia, Davide; Montanaro, Lucio; Arciola, Carla Renata

    2013-11-01

    Infection is currently regarded as the most severe and devastating complication associated to the use of biomaterials. The important social, clinical and economic impacts of implant-related infections are promoting the efforts to obviate these severe diseases. In this context, the development of anti-infective biomaterials and of infection-resistant surfaces is being regarded as the main strategy to prevent the establishment of implant colonisation and biofilm formation by bacteria. In this review, the attention is focused on the biomaterial-associated infections, from which the need for anti-infective biomaterials originates. Biomaterial-associated infections differ markedly for epidemiology, aetiology and severity, depending mainly on the anatomic site, on the time of biomaterial application, and on the depth of the tissues harbouring the prosthesis. Here, the diversity and complexity of the different scenarios where medical devices are currently utilised are explored, providing an overview of the emblematic applicative fields and of the requirements for anti-infective biomaterials. © 2013 Elsevier Ltd. All rights reserved.

  4. phytochemical screening of activity directed extracts of vernonia ...

    African Journals Online (AJOL)

    Admin

    Fractionation of the crude ethanolic extract of vernonia amygdalina using organic solvents of increasing polarities yielded activity directed fractions of benzene, chloroform, ethyl acetate, butanol, methanol and residue E. Phytochemical screening of the fractions show that there were significant differences (p≤0.05) ...

  5. Anti-bacterial activities and phytochemical screening of extracts of ...

    African Journals Online (AJOL)

    Anti-bacterial activity tests were carried out using disc diffusion assay and tube dilution technique, and phytochemical screening was carried out through Thin Layer Chromatography. The crude extracts showed antibacterial effects on M. vaccae, P. aeruginosa and B. subtilis. M. vaccae was most sensitive, particularly to the ...

  6. Phytochemical Screening and Antibacterial Activity of Cucurbita pepo

    African Journals Online (AJOL)

    Phytochemical screening and antibacterial activity of the extracts of Cucurbita pepo (backpeel and seeds) against Staphylococcus aureus and Salmonella typhi were carried out using standard procedures. The extraction was achieved using percolation method with ethanol and methanol as solvents. Higher yield of the ...

  7. Screening of various botanical extracts for antioxidant activity using ...

    African Journals Online (AJOL)

    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 ...

  8. Phytochemical screening and antimicrobial activity of roots, stem ...

    African Journals Online (AJOL)

    The roots, stem-bark and leaves of Grewia mollis which is used as herbal remedies for the cure of diarrhea and dysentery by natives in northern part of Nigeria were studied. The ethanol and water extracts of roots, stem-bark and leaves of the plant were subjected to phytochemical screening and antimicrobial activity against ...

  9. Phytochemical Screening and In Vitro Antitrypanosomal Activity of ...

    African Journals Online (AJOL)

    Phytochemical Screening and In Vitro Antitrypanosomal Activity of the Aerial Parts of Artemisia abyssinica Against Trypanosoma congolense Field Isolate. ... of infected blood and extracts at concentrations of 4, 2 and 0.4 mg/ml coupled with infectivity test in which a mixture of infected blood was inoculated to healthy mice.

  10. Further screening of Venda medicinal plants for activity against HIV ...

    African Journals Online (AJOL)

    The use of medicinal plants for AIDS-related conditions is common in South Africa. In order to establish an antiviral rationale for the use of these plants we screened fractions of the methanol extracts of medicinal plants for activity against HIV-1 reverse transcriptase (RT) and integrase (IN). The n-butanol fraction obtained ...

  11. Pitfalls using tributyrin agar screening to detect lipolytic activity in ...

    African Journals Online (AJOL)

    The metagenomics approach is an efficient method for obtaining novel biocatalysts and useful genes from uncultured microorganisms within diverse environments. In this study, we constructed a metagenomic library using a South African deep mine biofilm sample. The library was screened for lipolytic activity using LB ...

  12. Screening on Gibberellic Acid Producing Activity of Azospirillum Isolates

    International Nuclear Information System (INIS)

    Shun Lai Ei; Khin Mya Lwin; Myo Myint

    2010-12-01

    Six strains of Azopirillum spp were isolated from rice, sugarcane, corn, maize, sunflower and pepper roots and screened the gibberellic acid productivity. Only three strains of Azospirillum species showed the activity and were indentified by cultural, biochemical and drug sensitivity patterns. Among them,one strain isolated from rice root can produce microbial gibberellic acid. It showed greenish yellow colour in chromatogram under UV absorption. This screening method was studied from 1 to 14 days incubation. Qualitative measurement of GA productivity was determined by thin layer chromatography.

  13. Projection type transparent 3D display using active screen

    Science.gov (United States)

    Kamoshita, Hiroki; Yendo, Tomohiro

    2015-05-01

    Equipment to enjoy a 3D image, such as a movie theater, television and so on have been developed many. So 3D video are widely known as a familiar image of technology now. The display representing the 3D image are there such as eyewear, naked-eye, the HMD-type, etc. They has been used for different applications and location. But have not been widely studied for the transparent 3D display. If transparent large 3D display is realized, it is useful to display 3D image overlaid on real scene in some applications such as road sign, shop window, screen in the conference room etc. As a previous study, to produce a transparent 3D display by using a special transparent screen and number of projectors is proposed. However, for smooth motion parallax, many projectors are required. In this paper, we propose a display that has transparency and large display area by time multiplexing projection image in time-division from one or small number of projectors to active screen. The active screen is composed of a number of vertically-long small rotate mirrors. It is possible to realize the stereoscopic viewing by changing the image of the projector in synchronism with the scanning of the beam.3D vision can be realized by light is scanned. Also, the display has transparency, because it is possible to see through the display when the mirror becomes perpendicular to the viewer. We confirmed the validity of the proposed method by using simulation.

  14. Activity screening of environmental metagenomic libraries reveals novel carboxylesterase families

    Science.gov (United States)

    Popovic, Ana; Hai, Tran; Tchigvintsev, Anatoly; Hajighasemi, Mahbod; Nocek, Boguslaw; Khusnutdinova, Anna N.; Brown, Greg; Glinos, Julia; Flick, Robert; Skarina, Tatiana; Chernikova, Tatyana N.; Yim, Veronica; Brüls, Thomas; Paslier, Denis Le; Yakimov, Michail M.; Joachimiak, Andrzej; Ferrer, Manuel; Golyshina, Olga V.; Savchenko, Alexei; Golyshin, Peter N.; Yakunin, Alexander F.

    2017-01-01

    Metagenomics has made accessible an enormous reserve of global biochemical diversity. To tap into this vast resource of novel enzymes, we have screened over one million clones from metagenome DNA libraries derived from sixteen different environments for carboxylesterase activity and identified 714 positive hits. We have validated the esterase activity of 80 selected genes, which belong to 17 different protein families including unknown and cyclase-like proteins. Three metagenomic enzymes exhibited lipase activity, and seven proteins showed polyester depolymerization activity against polylactic acid and polycaprolactone. Detailed biochemical characterization of four new enzymes revealed their substrate preference, whereas their catalytic residues were identified using site-directed mutagenesis. The crystal structure of the metal-ion dependent esterase MGS0169 from the amidohydrolase superfamily revealed a novel active site with a bound unknown ligand. Thus, activity-centered metagenomics has revealed diverse enzymes and novel families of microbial carboxylesterases, whose activity could not have been predicted using bioinformatics tools. PMID:28272521

  15. INDUSTRIAL/MILITARY ACTIVITY-INITIATED ACCIDENT SCREENING ANALYSIS

    Energy Technology Data Exchange (ETDEWEB)

    D.A. Kalinich

    1999-09-27

    Impacts due to nearby installations and operations were determined in the Preliminary MGDS Hazards Analysis (CRWMS M&O 1996) to be potentially applicable to the proposed repository at Yucca Mountain. This determination was conservatively based on limited knowledge of the potential activities ongoing on or off the Nevada Test Site (NTS). It is intended that the Industrial/Military Activity-Initiated Accident Screening Analysis provided herein will meet the requirements of the ''Standard Review Plan for the Review of Safety Analysis Reports for Nuclear Power Plants'' (NRC 1987) in establishing whether this external event can be screened from further consideration or must be included as a design basis event (DBE) in the development of accident scenarios for the Monitored Geologic Repository (MGR). This analysis only considers issues related to preclosure radiological safety. Issues important to waste isolation as related to impact from nearby installations will be covered in the MGR performance assessment.

  16. 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... tract, gastrointestinal infections and waterborne diseases, has been included. The aim of the present study was to identify potential marine sources based on antimicrobial assay. ___________ *Corresponding author Telephone: 91(0)832 2450392 Fax...

  17. Starch-Chitosan Polyplexes: A Versatile Carrier System for Anti-Infectives and Gene Delivery

    Directory of Open Access Journals (Sweden)

    Hanzey Yasar

    2018-03-01

    Full Text Available Despite the enormous potential of nanomedicine, the search for materials from renewable resources that balance bio-medical requirements and engineering aspects is still challenging. This study proposes an easy method to make nanoparticles composed of oxidized starch and chitosan, both isolated from natural biopolymers. The careful adjustment of C/N ratio, polymer concentration and molecular weight allowed for tuning of particle characteristics. The system’s carrier capability was assessed both for anti-infectives and for nucleic acid. Higher starch content polyplexes were found to be suitable for high encapsulation efficiency of cationic anti-infectives and preserving their bactericidal function. A cationic carrier was obtained by coating the anionic polyplex with chitosan. Coating allowed for a minimal amount of cationic polymer to be employed and facilitated plasmid DNA loading both within the particle core and on the surface. Transfection studies showed encouraging result, approximately 5% of A549 cells with reporter gene expression. In summary, starch-chitosan complexes are suitable carriers with promising perspectives for pharmaceutical use.

  18. Screening and characterization of microorganisms with FR901379 acylase activity.

    Science.gov (United States)

    Ueda, Satoshi; Sakamoto, Kazunori; Oohata, Nobutaka; Tsuboi, Masaru; Yamashita, Michio; Hino, Motohiro; Yamada, Masato; Hashimoto, Seiji

    2010-02-01

    A simple and rapid screen was performed for microorganisms producing cyclic lipopeptide acylase, an enzyme that deacylates the acyl side chain of FR901379 to yield a cyclic peptide, FR179642, which is an important intermediate in producing micafungin. Among approximately 3800 newly isolated strains from soil samples, 5 microorganisms expressing high acylase activity were selected and classified, 3 as Streptomyces spp. and 2 as filamentous fungi. This is the first time that these strains have been identified as cyclic lipopeptide acylase producers. Both fungi and streptomycetes showed differing optimum pH and temperature profiles for acylase activity.

  19. How Children Use Active Videogames and the Association Between Screen Time and Physical Activity.

    Science.gov (United States)

    Forde, Cuisle; Hussey, Juliette

    2015-08-01

    The energy required to play active videogames (AVGs) has been reported on in the literature; however, little is known about how children use such games in their home environment. The aim of this study was to investigate children's use of AVGs and the association among AVG use, other screen-based activities, and physical activity levels. Eight hundred and twenty children 12.1 (0.6) years of age participated. Physical activity levels, sedentary screen-based activities, and AVG use were investigated. Differences across genders and deprivation indices were also analyzed. Fifty-eight percent of children met minimal physical activity guidelines. Forty-seven percent of children exceeded screen time recommendations. Of those who had access to AVGs, more children played sedentary games (or active games in a sedentary manner [68 percent]) than active games (55 percent) on AVG consoles. Furthermore, sedentary games were played for longer than active games. AVG play was positively correlated with reported time spent watching television (P=0.02). In free-living conditions AVG consoles are being used by more children and for longer durations as sedentary screen-based devices rather than active screen-based devices.

  20. Preparation of ZnO/Ag nanocomposite and coating on polymers for anti-infection biomaterial application

    Science.gov (United States)

    Sadeghi, Babak

    2014-01-01

    ZnO/Ag nanocomposites coated with polyvinyl chloride (PVC) were prepared by chemical reduction method, for anti-infection biomaterial application. There is a growing interest in attempts in using biomolecular as the templates to grow inorganic nanocomposites in controlled morphology and structure. By optimizing the experiment conditions, we successfully fabricated high yield of ZnO/Ag nanocomposite with full coverage of high-density polyvinyl chloride (PVC) coating. More importantly, ZnO/Ag nanocomposites were shown to significantly inhibit the growth of Staphylococcus aureus in solution. It was further shown that ZnO/Ag nanocomposites induced thiol depletion that caused death of S. aureus. The coatings were fully characterized using techniques such as scanning electron microscopy (SEM), transmission electron microscopy (TEM) and X-ray diffraction (XRD). Most importantly, compared to uncoated metals, the coatings on PVC promoted healthy antibacterial activity. Importantly, compared to ZnO-Ag -uncoated PVC, the ZnO/Ag nanocomposites coated was approximately triplet more effective in preventing bacteria attachment. The result of Thermal Gravimetric Analysis (TGA) indicates that, the ZnO/Ag nanocomposites are chemically stable in the temperature range from 50 to 900 °C. This result, for the first time, demonstrates the potential of using ZnO/Ag nanocomposites as a coating material for numerous anti-bacterial applications.

  1. Preparation of ZnO/Ag nanocomposite and coating on polymers for anti-infection biomaterial application.

    Science.gov (United States)

    Sadeghi, Babak

    2014-01-24

    ZnO/Ag nanocomposites coated with polyvinyl chloride (PVC) were prepared by chemical reduction method, for anti-infection biomaterial application. There is a growing interest in attempts in using biomolecular as the templates to grow inorganic nanocomposites in controlled morphology and structure. By optimizing the experiment conditions, we successfully fabricated high yield of ZnO/Ag nanocomposite with full coverage of high-density polyvinyl chloride (PVC) coating. More importantly, ZnO/Ag nanocomposites were shown to significantly inhibit the growth of Staphylococcus aureus in solution. It was further shown that ZnO/Ag nanocomposites induced thiol depletion that caused death of S. aureus. The coatings were fully characterized using techniques such as scanning electron microscopy (SEM), transmission electron microscopy (TEM) and X-ray diffraction (XRD). Most importantly, compared to uncoated metals, the coatings on PVC promoted healthy antibacterial activity. Importantly, compared to ZnO-Ag -uncoated PVC, the ZnO/Ag nanocomposites coated was approximately triplet more effective in preventing bacteria attachment. The result of Thermal Gravimetric Analysis (TGA) indicates that, the ZnO/Ag nanocomposites are chemically stable in the temperature range from 50 to 900°C. This result, for the first time, demonstrates the potential of using ZnO/Ag nanocomposites as a coating material for numerous anti-bacterial applications. Copyright © 2013 Elsevier B.V. All rights reserved.

  2. 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 (Panalgesic effect in all test methods (hot plate, acetic acid-induced writhing and formalin). The analgesic activity was compared with a standard drug (ketorolac at 10 mg/kg). Based on the present findings and previous literature review it can be concluded that flavonoids 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.

  3. 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.

  4. Reporter Gene-Based Screening for TPP Riboswitch Activators.

    Science.gov (United States)

    Lünse, Christina E; Mayer, Günter

    2017-01-01

    With the rise of multidrug resistant bacteria and a growing number of nosocomial infections, there has been an increased interest in finding new antibacterial drugs and drug targets. Riboswitches represent attractive new antibacterial drug targets, because they not only inherently recognize a specific metabolite or ion with their RNA aptamer domain, but also often regulate essential metabolic pathways. Here, we describe a reporter gene-based screen to identify compounds that activate the thiamine pyrophosphate (TPP) riboswitch in bacteria. This assay can be easily adapted for different riboswitch classes and thus has the potential to target many essential metabolic pathways and a broad spectrum of bacterial pathogens.

  5. 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.

  6. 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.

  7. Phytochemicals Screening and Antioxidant Activity of Annona muricata Aqueous Extracts

    International Nuclear Information System (INIS)

    Rosniza Razali; Hazlina Ahmad Hassali; Arapoc, D.J.

    2016-01-01

    Annona Muricata belongs to the family Annonaceae which is known to have anticancer, anti-inflammatory and many other bio activities. Leaves, twig, fruit and seed of A. muricata were collected from Suhan Biotech and dried. Hot and cold aqueous extracts were prepared for the preliminary screening of phytochemicals and aqueous extracts of A. muricata were evaluated for total phenolic, scavenging assay (DPPH; 1-1-diphenyl-2-picrylhydrazyl) and cytotoxic activities. Phytochemicals screening of leaves extracts revealed the presence of alkaloids, terpenoid, reducing sugar, carbohydrate and anthocyanins. While for twig extracts it revealed the presence of coumarine. Antra quinones, terpenoid, flavonoid, reducing sugar, lipids and coumarine were found in fruit and seed extracts. The total phenolic content was found to be 2.372±0.922 μg GAE/ g, 85.85±6.23 μg GAE/ g, 53.56±8.39 μg GAE/ g and 54.67±13.33 μg GAE/ g for leaves, twig, fruit and seed respectively. On the other hand, all extract have showed IC 50 value more than 500 μg/ mL in DPPH scavenging assay. Cytotoxic evaluation of all extracts against HTB43, MCF-7 and MDAMB231 cell lines showed IC 50 value more than 250 μg/ mL. In conclusion, the results showed that aqueous extract of A.muricata was inappropriate as anticancer agen (author)

  8. Screening of Brazilian medicinal plants for antiviral activity against rotavirus.

    Science.gov (United States)

    Cecílio, Alzira Batista; de Faria, Déborah Behr; Oliveira, Pollyana de Carvalho; Caldas, Sérgio; de Oliveira, Dario Alves; Sobral, Marcos Eduardo Guerra; Duarte, Maria Gorette Resende; Moreira, Carolina Paula de Souza; Silva, Cláudia Gontijo; de Almeida, Vera Lúcia

    2012-06-14

    Brazilian medicinal plants traditionally used for the treatment of diarrhoea were investigated for their in vitro antiviral activity against the simian rotavirus SA11. The ethanolic crude extracts of plants collected in the cerrado of Minas Gerais, Brazil were submitted to phytochemical screening. The cytotoxicity of the extracts was inferred by cellular morphologic alterations. Antiviral activity was assessed by the ability of the extracts to inhibit the cytopathic effect (CPE) of rotavirus on the treated cells. RT-PCR was performed to confirm and/or confront antiviral assay data. The maximum non-toxic concentration ranged from 50 to 500 μg/mL. All extracts were toxic at a concentration of 5000 μg/mL but no extract showed cytotoxicity at 50 μg/mL. The species Byrsonima verbascifolia, Myracrodruon urundeuva, Eugenia dysenterica and Hymenaea courbaril exhibited the strongest in vitro activity against rotavirus. Their extracts prevented the formation of CPE, and RT-PCR analysis detected no amplification of genetic material from rotavirus. Tannins, flavonoids, saponins, coumarins and terpenes were the major classes of natural products found in the leaf extracts that showed antiviral activity. Among the species studied, Byrsonima verbascifolia, Eugenia dysenterica, Hymenaea courbaril and Myracrodruon urundeuva showed potential activity against rotavirus and are worthy of further study. The present study corroborates ethnopharmacological data as a valuable source in the selection of plants with antiviral activity and to some extent validates their traditional uses. Published by Elsevier Ireland Ltd.

  9. Phytochemical Screening, Antimicrobial and Antioxidant Activities of Ficus natalensis

    International Nuclear Information System (INIS)

    Ajaib, M.

    2016-01-01

    Phytochemical screening, antimicrobial and antioxidant potential of the bark and leaves extracts of Ficus natalensis were carried out by using various techniques. Phytochemical analysis showed the presence of terpenoids, alkaloids, flavonoids, tannins, saponins, cardiac glycosides and reducing sugars in different extracts of Ficus natalensis. The antibacterial potential against S. aureus was reported as most promising amongst all. The petroleum ether extract of leaves with a zone of inhibition 50 ± 0.51 mm and bark extracts with a zone of inhibition 55.7 ± 1.15 mm inhibited S. aureus. The chloroform leaves extract also showed an inhibition zone of 50 ± 2 mm against S. aureus. The antifungal potential of methanol bark extract at 43.7 ±1.527 mm and petroleum ether extracts of bark with zones of inhibition 37 ± 0.577 mm against A. niger showed most prominent activity. By using different assays, the extracts were screened for the antioxidant potential. The estimation of antioxidant activity by metal chelating activity revealed that water extract of leaves was most active with a value of 74.673 ± 0.302 percentage bound iron. The chloroform extract of bark showed highest flavonoid content (1005.53 ± 0.503 mg/mL of quercetin), whereas chloroform extract of leaves exhibited maximum phenolic content (21.626 ± 0.545 mg/g of GAE). In ABTS assay, water extract of leaves showed maximum TEAC value (7.713 ± 0.7 mM of trolox equivalent). The highest free radical scavenging DPPH percentage was observed with distilled water extract of bark (91.92 ± 0.08 percent). (author)

  10. 77 FR 12063 - Joint Meeting of the Anti-Infective Drugs Advisory Committee and the Nonprescription Drugs...

    Science.gov (United States)

    2012-02-28

    ... DEPARTMENT OF HEALTH AND HUMAN SERVICES Food and Drug Administration [Docket No. FDA-2012-N-0001] Joint Meeting of the Anti-Infective Drugs Advisory Committee and the Nonprescription Drugs Advisory Committee; Notice of Meeting AGENCY: Food and Drug Administration, HHS. ACTION: Notice. This notice announces a forthcoming meeting of a public...

  11. Modulation of Quorum Sensing in a Gram Positive Pathogen by Linear Imprinted Copolymers with anti-Infective Properties

    NARCIS (Netherlands)

    Motib, Anfal; Guerreiro, Antonio; Al-Bayati, Firas; Piletska, Elena; Manzoor, Irfan; Shafeeq, Sulman; Kadam, Anagha; Kuipers, Oscar; Hiller, Luisa; Cowen, Todd; Piletsky, Sergey; Andrew, Peter; Yesilkaya, Hasan

    2017-01-01

    Here we describe the development, characterization and biological testing of a new type of linear molecularly imprinted polymer (LMIP) designed to act as anti-infective by blocking the quorum sensing (QS) mechanism and so preventing virulence of the pathogen Streptococcus pneumoniae. The LMIP is

  12. 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.

  13. [Physical activity, screen time and sleep patterns in Chilean girls].

    Science.gov (United States)

    Aguilar, M M; Vergara, F A; Velásquez, E J A; García-Hermoso, A

    2015-11-01

    Physical activity (PA), screen time (ST), and sleep are modifiable lifestyle habits for health. The objectives of this study were: a) to examine the association between PA, ST, and both, on sleep patterns; and b) to determine the influence of PA and ST on sleep problems in Chilean girls. The study involved 196 children (12.2 years). Patterns and sleep problems were assessed using the Spanish version of the Sleep Self-Report, and the PA through the Physical Activity Questionnaire for Adolescents (PAQ-A), both in Castilian. The ST was assessed using several questions about television, game console and computer use. The ST recommendation (2h a day) was exceeded by 63.2% of the girls. In general, the most active girls (last quartile) that did not exceed the recommendations of ST reported higher sleep quality and total score values compared to those who did not meet both. The logistic regression analysis showed that girls who did not meet both habits were more likely to have sleep quality (odds ratio=17.8, P=.018), and general sleep problems (odds ratio=7.85, P=.025). Parents need to set limits on sedentary leisure time and encourage more active habits, as sleep is a parameter closely linked to a better health profile in youth. Copyright © 2014 Asociación Española de Pediatría. Published by Elsevier España, S.L.U. All rights reserved.

  14. Parents' perception of neighbourhood environment as a determinant of screen time, physical activity and active transport.

    Science.gov (United States)

    Carson, Valerie; Kuhle, Stefan; Spence, John C; Veugelers, Paul J

    2010-01-01

    To study the importance of parents' perception of neighbourhood environment for health behaviours such as screen time, physical activity, and active transport in a Canadian context. As part of the REAL Kids Alberta project, 3,421 grade five students from 148 randomly selected schools in Alberta and their parents were surveyed in the spring of 2008. Physical activity was assessed by self-report using an adapted version of the Physical Activity Questionnaire for Older Children (PAQ-C). Screen time and active transport (walking and biking) was assessed by parent proxy reports. Parents were also surveyed on their perception of their neighbourhoods. These responses were reduced to three components (satisfaction/services, safety, sidewalks/parks) through principal component analysis. Subsequent multilevel logistic regression analyses were conducted to quantify the associations of these principal neighbourhood components with screen time, physical activity, and active transport. Children residing in neighbourhoods with good satisfaction/services and sidewalks/parks were significantly more likely to engage in 2 hours or less of screen time and to be physically active. Children in neighbourhoods with good sidewalks/parks were also more likely to engage in active transport to and from school. However, perceived neighbourhood safety had little impact on activity. The findings suggest physical activity and active transport may be increased and sedentary behaviours reduced through 1) increasing access to parks, playgrounds, and play spaces, 2) increasing access to sports and recreation programs, and 3) provision of sidewalks such that children and youth can walk or bike to school.

  15. In Vitro Screening for Cytotoxic Activity of Herbal Extracts

    Directory of Open Access Journals (Sweden)

    Valter R. M. Lombardi

    2017-01-01

    Full Text Available Experimental studies have shown that a variety of chemopreventive plant components affect tumor initiation, promotion, and progression and the main difference, between botanical medicines and synthetic drugs, resides in the presence of complex metabolite mixtures shown by botanical medicine which in turn exert their action on different levels and via different mechanisms. In the present study, we performed an in vitro screening of ethanol extracts from commercial plants in order to investigate potential antitumor activity against human tumor cell lines. Experimental results obtained through a variety of methods and techniques indicated that extracts of I. verum, G. glabra, R. Frangula, and L. usitatissimum present significant reduction in in vitro tumor cell proliferation, suggesting these extracts as possible chemotherapeutical adjuvants for different cancer treatments.

  16. Virulence evolution in response to anti-infection resistance: toxic food plants can select for virulent parasites of monarch butterflies.

    Science.gov (United States)

    de Roode, J C; de Castillejo, C Lopez Fernandez; Faits, T; Alizon, S

    2011-04-01

    Host resistance to parasites can come in two main forms: hosts may either reduce the probability of parasite infection (anti-infection resistance) or reduce parasite growth after infection has occurred (anti-growth resistance). Both resistance mechanisms are often imperfect, meaning that they do not fully prevent or clear infections. Theoretical work has suggested that imperfect anti-growth resistance can select for higher parasite virulence by favouring faster-growing and more virulent parasites that overcome this resistance. In contrast, imperfect anti-infection resistance is thought not to select for increased parasite virulence, because it is assumed that it reduces the number of hosts that become infected, but not the fitness of parasites in successfully infected hosts. Here, we develop a theoretical model to show that anti-infection resistance can in fact select for higher virulence when such resistance reduces the effective parasite dose that enters a host. Our model is based on a monarch butterfly-parasite system in which larval food plants confer resistance to the monarch host. We carried out an experiment and showed that this environmental resistance is most likely a form of anti-infection resistance, through which toxic food plants reduce the effective dose of parasites that initiates an infection. We used these results to build a mathematical model to investigate the evolutionary consequences of food plant-induced resistance. Our model shows that when the effective infectious dose is reduced, parasites can compensate by evolving a higher per-parasite growth rate, and consequently a higher intrinsic virulence. Our results are relevant to many insect host-parasite systems, in which larval food plants often confer imperfect anti-infection resistance. Our results also suggest that - for parasites where the infectious dose affects the within-host dynamics - vaccines that reduce the effective infectious dose can select for increased parasite virulence.

  17. Screening of solvent dependent antibacterial activity of Prunus domestica.

    Science.gov (United States)

    Yaqeen, Zahra; Naqvi, Naim-ul-Hasan; Sohail, Tehmina; Rehman, Zakir-ur; Fatima, Nudrat; Imran, Hina; Rehman, Atiqur

    2013-03-01

    Fruit of Prunus domestica was extracted in ethanol. The ethanol extract was further extracted with two solvents ethyl acetate and chloroform. The crude ethanol extract and two fractions (ethyl acetate and chloroform) were screened for their antibacterial activity using the agar well diffusion method .They were tested against nine bacteria; five Gram positive bacteria (Staphylococcus aureus, Streptococcuc intermedius, Bacillus cereus, Bacillus pumilus) and four Gram negative bacteria (Eschrichia coli, Proteus mirabilis Shigella flexneri, Salmonella typhi and Klebsiela pneumoniae). The susceptibility of microorganisms to all three fractions was compared with each other and with standard antibiotic (Ampicillin) Among all fractions ethyl acetate exhibited highest antibacterial activity (average zone of inhibition 34.57mm ± 1.3) while ethyl alcohol exhibited least antibacterial activity (average zone of inhibition 17.42mm ± 3.3). Minimum inhibitory concentration of ethanol, ethyl acetate and chloroform fractions was found in the range of 78 μ g/ml to 2500 μ gl/ml against gram positive and gram negative bacteria.

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

    International Nuclear Information System (INIS)

    Frank, C.W.; Anderson, T.D.; Cooley, C.R.; Hain, K.E.; Lien, S.C.T.; Erickson, M.D.

    1991-01-01

    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

  19. Is a Perceived Activity-Friendly Environment Associated with More Physical Activity and Fewer Screen-Based Activities in Adolescents?

    NARCIS (Netherlands)

    Kopcakova, Jaroslava; Veselska, Zuzana Dankulincova; Geckova, Andrea Madarasova; Bucksch, Jens; Nalecz, Hanna; Sigmundova, Dagmar; van Dijk, Jitse P.; Reijneveld, Sijmen A.

    2017-01-01

    Background: The aim of this study is to explore if perception of an activity-friendly environment is associated with more physical activity and fewer screen-based activities among adolescents. Methods: We collected self-reported data in 2014 via the Health Behavior in School-aged Children

  20. 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.

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

    International Nuclear Information System (INIS)

    Kaklamani, Georgia; Bowen, James; Mehrban, Nazia; Dong, Hanshan; Grover, Liam M.; Stamboulis, Artemis

    2013-01-01

    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 2 /H 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.

  2. 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.

  3. 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

  4. Anti-infective strategies of the future: is there room for species-specific antibacterial agents?

    Science.gov (United States)

    Then, Rudolf L; Sahl, Hans-Georg

    2010-01-01

    Broad-spectrum antibiotics, directed against conserved bacterial targets, are the mainstay of antibacterial therapy. Increasing resistance, however, demands new strategies. Over time a number of therapeutic concepts have evolved, starting out with the use of polyclonal antisera, which were rapidly replaced by the easier to use antibiotics. Other concepts, such as immunotherapy, radioimmunotherapy, anti-virulence agents, phage therapy and others are under evaluation and often limited in application. In the discovery process of new antibiotics in the pharmaceutical industry quite a number of new agents have emerged, which exhibit a surprisingly high degree of species-specificity. None of them has been considered for development so far. Some examples from the literature which show selectivity for Helicobacter pylori, Pseudomonas aeruginosa, Haemophilus influenzae, Staphylococcus aureus, anaerobes, and others, will be discussed here. It is postulated that there is a room for such agents in future antibacterial therapy, e.g. in difficult to treat infections caused by nonfermenters such as multiresistant P. aerugoinosa, Acinetobacter, Enterobacteriaceae, and S.aureus, including MRSA. Their application would include monotherapy as well as combination therapy with other antibiotics, anti-virulence agents or immunotherapy and these possibilities would greatly expand the current anti-infective armamentarium.

  5. Screening antimicrobial activity of various extracts of Urtica dioica

    Directory of Open Access Journals (Sweden)

    Amir Modarresi-Chahardehi

    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.

  6. 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.

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

    Science.gov (United States)

    Tan, Jing; Li, Yiting; Liu, Zhiyuan; Qu, Shuxin; Lu, Xiong; Wang, Jianxin; Duan, Ke; Weng, Jie; Feng, Bo

    2015-07-01

    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.

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

    International Nuclear Information System (INIS)

    Tan, Jing; Li, Yiting; Liu, Zhiyuan; Qu, Shuxin; Lu, Xiong; Wang, Jianxin; Duan, Ke; Weng, Jie; Feng, Bo

    2015-01-01

    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 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

  9. 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.

  10. Active versus Passive Screen Time for Young Children

    Science.gov (United States)

    Sweetser, Penelope; Johnson, Daniel; Ozdowska, Anne; Wyeth, Peta

    2012-01-01

    In this paper we report some initial findings from our investigations into the Australian Government's Longitudinal Study of Australian Children dataset. It is revealed that the majority of Australian children are exceeding the government's Screen Time recommendations and that most of their screen time is spent as TV viewing, as opposed to video…

  11. Post-migration screening for active tuberculosis in Victoria, Australia.

    Science.gov (United States)

    Flynn, M; Brown, L; Tesfai, A; Lauer, T

    2012-01-01

    Tuberculosis (TB) screening clinic. To determine TB prevalence at entry, screening yield and incidence in immigrants on a TB health undertaking (TBU) who were selected for post-migration screening due to an abnormal chest radiograph (CXR) in Victoria, Australia, in the years 1996-2006. Rates of notified TB calculated from linkage of a screening programme database with the Victorian TB database. Prevalence at entry (cases notified between arrival in Australia and 6 months after the screening registration date) was 505 per 100,000 population; yield at entry (prevalent cases detected by the screening programme) was 420/100,000, and incidence (cases notified between 6 and 12 months after screening registration date) was 160/100,000 person-years. Persons issued a TBU after applying from within Australia (on-shore) had a prevalence of 1876/100,000, seven-fold higher than those issued a TBU outside Australia (off-shore, 254/100,000). The combination of an abnormal CXR and a tuberculin skin test ≥ 15 mm carried a prevalence of notified TB of 2907/100,000. Selective post-migration screening can achieve a high yield of notified TB.

  12. A screening method for cardiovascular active compounds in marine algae.

    Science.gov (United States)

    Agatonovic-Kustrin, S; Kustrin, E; Angove, M J; Morton, D W

    2018-05-18

    The interaction of bioactive compounds from ethanolic extracts of selected marine algae samples, separated on chromatographic plates, with nitric/nitrous acid was investigated. The nature of bioactive compounds in the marine algae extracts was characterised using UV absorption spectra before and after reaction with diluted nitric acid, and from the characteristic colour reaction after derivatization with anisaldehyde. It was found that diterpenes from Dictyota dichotoma, an edible brown algae, and sterols from green algae Caulerpa brachypus, bind nitric oxide and may act as a nitric oxide carrier. Although the carotenoid fucoxanthin, found in all brown marine algae also binds nitric oxide, the bonds between nitrogen and the fucoxanthin molecule are much stronger. Further studies are required to evaluate the effects of diterpenes from Dictyota dichotoma and sterols from green algae Caulerpa brachypus to see if they have beneficial cardiovascular effects. The method reported here should prove useful in screening large numbers of algae species for compounds with cardiovascular activity. Copyright © 2018 Elsevier B.V. All rights reserved.

  13. Anti-infective potential of a medicinal plant pimpenella stewartii used traditionally in hazara

    International Nuclear Information System (INIS)

    Gul, F.; Hassan, M.

    2016-01-01

    Medicinal plants have been used since long as folk medicines and also in Ayuvedic and Unani systems of treatment. They have importance to save human and animal lives because of their utilization in the herbal medicines. In all over the word plants are in constant use for curing of various kinds of diseases. The herbal medicines are effective due to presence of bioactive compounds along with vitamins and minerals in them. Moreover, plants produce photo-chemicals mainly secondary metabolites which have significant pharmaceutical activities like antioxidant, antimicrobial, pesticidal and anti-tumour activity. They are very effective and have little or no side effects. Methods: Five microbial strains including three fungal and two bacterial species were tested for the efficacy of plant materials by Agar diffusion method. The fungal species were Aspergilus flavus, Aspergilus niger and Alternaria alternata while bacterial species included Arvenia caratovora and Xanthomans spp. Results: Results obtained for methanolic extracts of Pimpenella stewartii against Aspergilus flavus, Aspergilus niger and Alternaria alternata showed significant antifungal activity. The antibacterial screening of Methanolic extracts of Pimpenella stewartii were evaluated against Arvenia caratovora and Xanthomans spp. The best zone of inhibition was found against Xanthomans spp (97.33 ± 2 mm) at 250 ppm concentration followed by Arvenia caratovora (49.7 ± 14 mm) at same concentration. (author)

  14. Screening of some marine plants from the Indian coast for biological activity

    Digital Repository Service at National Institute of Oceanography (India)

    Naqvi, S.W.A; Solimabi; Kamat, S.Y.; De; Reddy, C.V.G.; Bhakuni, D.S.; Dhawan, B

    Extracts of twenty five seaweeds from Indian coast have been put through a broad biological screen which includes tests for antiviral, antibacterial, antifungal, antiprotozoal, antifertility activities and a wide range of pharmacological activities...

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

    Science.gov (United States)

    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 predict MVPA, but support for PA did (positive association). The association between support and MVPA, moreover, varied as a function of permissive parenting. For parents high in permissiveness, the association was positive (greater support was related to greater MVPA and therefore protective). For parents low in permissiveness, the association was neutral; support did not matter. Authoritarian and permissive parenting styles were both associated with greater screen time. Conclusions: Parenting practices and styles should be considered jointly, offering implications for tailored interventions. PMID:24812256

  16. Predicting child physical activity and screen time: parental support for physical activity and general parenting styles.

    Science.gov (United States)

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

    2014-07-01

    To examine relationships between parenting styles and practices and child moderate-to-vigorous physical activity (MVPA) and screen time. 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. Parenting style did not predict MVPA, but support for PA did (positive association). The association between support and MVPA, moreover, varied as a function of permissive parenting. For parents high in permissiveness, the association was positive (greater support was related to greater MVPA and therefore protective). For parents low in permissiveness, the association was neutral; support did not matter. Authoritarian and permissive parenting styles were both associated with greater screen time. Parenting practices and styles should be considered jointly, offering implications for tailored interventions. © The Author 2014. Published by Oxford University Press on behalf of the Society of Pediatric Psychology. All rights reserved. For permissions, please e-mail: journals.permissions@oup.com.

  17. Phytochemical Screening and Mosquito Repellent Activity of the ...

    African Journals Online (AJOL)

    The phytochemical screening of extracts from Euphorbia balsamifera was carried out, and the results revealed that the stem bark contains alkaloids, tannins, flavonoids, saponins, glycosides, terpenoids and sterols. The ethanol extract of the stem bark of Euphorbia balsamifera (commonly known as Ayyara in Hausa) was ...

  18. Phytochemical Screening and Antibacterial Activity of stem bark ...

    African Journals Online (AJOL)

    This study evaluated the phytochemical constituents and the antimicrobial properties of the ethanolic extract of the stem bark of Alstonia boonei, a plant used for the treatment of wounds and urinary tract infections in Nigeria. Phytochemical screening was done using standard methods while the agar well diffusion method ...

  19. Screening for Biological Activity of Solanum incanum and Conyza ...

    African Journals Online (AJOL)

    The isolated Rabbit jejunum smooth muscle contraction assay was used to screen two Kenyan medicinal plants; Solanum incanum and Conyza sumatrensis used to treat/relieve constipation. Cold and Heat extraction methods were used to prepare the plant extracts from freshly collected root and stem barks of S. incanum ...

  20. Screen-based activities and physical complaints among adolescents from the Nordic countries

    Directory of Open Access Journals (Sweden)

    Bjarnason Thoroddur

    2010-06-01

    Full Text Available Abstract Background A positive association between time spent on sedentary screen-based activities and physical complaints has been reported, but the cumulative association between different types of screen-based activities and physical complaints has not been examined thoroughly. Methods The cross-sectional association between screen-based activity and physical complaints (backache and headache among students was examined in a sample of 31022 adolescents from Denmark, Sweden, Norway, Finland, Iceland and Greenland, as part of the Health behaviour in school-aged children 2005/06 (HBSC study. Daily hours spent on screen-based activities and levels of physical complaints were assessed using self-reports. Results Logistic regression analysis indicated that computer use, computer gaming and TV viewing contributed uniquely to prediction of weekly backache and headache. The magnitude of associations was consistent across types of screen based activities, and across gender. Conclusion The observed associations indicate that time spent on screen-based activity is a contributing factor to physical complaints among young people, and that effects accumulate across different types of screen-based activities.

  1. 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...

  2. Breast cancer screening in Italy: evaluating key performance indicators for time trends and activity volumes.

    Science.gov (United States)

    Giordano, Livia; Castagno, Roberta; Giorgi, Daniela; Piccinelli, Cristiano; Ventura, Leonardo; Segnan, Nereo; Zappa, Marco

    2015-01-01

    Together with the National centre for screening monitoring (ONS), GISMa supports annual collection of data on national breast screening activities. Aggregated data on implementation and performance are gathered through a standardized form to calculate process and impact indicators. Analyzed data belong to 153 local programmes in the period 2006-2011 (2006-2012 for participation rate only). During the whole period, Italian crude participation rate exceeded GISMa's acceptable standard (50%), even though a higher participation in northern and central Italy compared to southern Italy and Islands was observed. Time trend analysis of diagnostic indicators confirmed in 2011 an adequate quality of breast screening performance, especially at subsequent screening. Recall rate at initial screening did not reach the acceptable standard (performance was achieved at subsequent screening. The same trend was followed by the overall detection rate and positive predictive value. They both showed a progressive reduction (from 6.2‰ in 2006 to 4.5‰ in 2011 for DR and from 8.0% in 2006 to 5.2% in 2011 for PPV, respectively) at initial screening and a good, stable trend at subsequent screening. Activity volume analysis shows that in programmes with greater activity (test/year ≥10,000) RR at both initial and subsequent screening has a better performance. This is also true for DR and PPV where programmes with high volumes of activity do better, especially when compared with those that interpret fewer than 5,000 mammograms per year. In spite of a few limits, these results are reassuring, and they reward the efforts made by screening professionals. It is therefore important to continue to monitor screening indicators and suggest, test, and evaluate new strategies for continuous improvement.

  3. Relationship of weight status, physical activity and screen time with academic achievement in adolescents.

    Science.gov (United States)

    García-Hermoso, Antonio; Marina, Raquel

    The aim of this study was to examine the relationship of weight status, physical activity and screen time with academic achievement in Chilean adolescents. The present cross-sectional study included 395 adolescents. The International Obesity Task Force cut-off points were used to define the weight status. Physical activity was assessed using the Physical Activity Questionnaire for Adolescents and screen time was assessed using several questions about television, videogame and computer use. Academic achievement was measured using the mean of the grades obtained in mathematics and language subjects. In both genders, adolescents with obesity and excessive screen time earned worse grades compared to their non-obese peers and their peers that complied with screen time recommendations. The logistic regression analysis showed that adolescents with obesity, classified with medium-low physical activity and excessive screen time recommendations (excess ≥2h/day) are less likely to obtain high academic achievement (boys: OR=0.26; girls: OR=0.23) compared to their non-obese peers, high levels of physical activity and those who comply with the current screen time recommendations. Similar results were observed in adolescents with obesity and classified with medium-low physical activity (boys: OR=0.46; girls: OR=0.33) or excessive screen time (boys: OR=0.35; girls: OR=0.36) compared to adolescents with high levels of physical activity and those who complied with the screen time recommendations, respectively. This study shows that when combined, obesity, low-medium levels of physical activity and excessive screen time might be related to poor academic achievement. Copyright © 2015 Asia Oceania Association for the Study of Obesity. Published by Elsevier Ltd. All rights reserved.

  4. Synthesis of thiazolium salts and their screening for catalytic activity

    Energy Technology Data Exchange (ETDEWEB)

    Lee, Seul Ki; Kim, Do Joong; Park, Jin Kyoon [Dept. of Chemistry and Institute of Functional Materials, Pusan National University, Busan (Korea, Republic of)

    2015-05-15

    A facile synthetic method to prepare thiazolium-based ionic liquids in high yield was developed. The direct alkylation of thiazole was performed using a trialkyl orthoester as both the alkyl donor and the solvent. The synthesized thiazolium salts were subsequently screened for their ability to catalyze the benzoin condensation reaction. Of the salts that were tested, 3-butyl,4,5-dimethyl thiazolium salt, was found to be the best catalyst.

  5. Phytochemical Screening and Aphrodisiac Activity of Asparagus racemosus

    OpenAIRE

    Javeed Ahmed Wani; Rajeshwara N. Achur; R. K. Nema

    2011-01-01

    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 aphr...

  6. Cost-effectiveness of screening for active cases of tuberculosis in Flanders, Belgium.

    Science.gov (United States)

    Smit, G Suzanne A; Apers, Ludwig; Arrazola de Onate, Wouter; Beutels, Philippe; Dorny, Pierre; Forier, An-Marie; Janssens, Kristien; Macq, Jean; Mak, Ruud; Schol, Sandrina; Wildemeersch, Dirk; Speybroeck, Niko; Devleesschauwer, Brecht

    2017-01-01

    To assess the cost-effectiveness of the tuberculosis screening activities currently funded by the Flemish government in Flanders, Belgium. After estimating the expenses for 2013-2014 of each of nine screening components - which include high-risk groups, contacts and people who are seeking tuberculosis consultation at a centre for respiratory health care - and the associated costs per active case of tuberculosis identified between 2007 and 2014, we compared the cost-effectiveness of each component. The applied perspective was that of the Flemish government. The three most cost-effective activities appeared to be the follow-up of asylum seekers who were found to have abnormal X-rays in initial screening at the Immigration Office, systematic screening in prisons and contact investigation. The mean costs of these activities were 5564 (95% uncertainty interval, UI: 3791-8160), 11 603 (95% UI: 9010-14 909) and 13 941 (95% UI: 10 723-18 201) euros (€) per detected active case, respectively. The periodic or supplementary initial screening of asylum seekers and the screening of new immigrants from high-incidence countries - which had corresponding costs of €51 813 (95% UI: 34 855-76 847), €126 236 (95% UI: 41 984-347 822) and €418 359 (95% UI: 74 975-1 686 588) - appeared much less cost-effective. Between 2007 and 2014, no active tuberculosis cases were detected during screening in the juvenile detention centres. In Flanders, tuberculosis screening in juvenile detention centres and among new immigrants and the periodic or supplementary initial screening of asylum seekers appear to be relatively expensive ways of detecting people with active tuberculosis.

  7. Anti-infective effects of Brazilian Caatinga plants against pathogenic bacterial biofilm formation.

    Science.gov (United States)

    Silva, Laura Nunes; Trentin, Danielle da Silva; Zimmer, Karine Rigon; Treter, Janine; Brandelli, Clara Lia Costa; Frasson, Amanda Piccoli; Tasca, Tiana; da Silva, Alexandre Gomes; da Silva, Márcia Vanusa; Macedo, Alexandre José

    2015-03-01

    The local communities living in the Brazilian Caatinga biome have a significant body of traditional knowledge on a considerable number of medicinal plants used to heal several maladies. Based on ethnopharmacological data, this study screened 23 aqueous plant extracts against two well-known models of biofilm-forming bacteria: Staphylococcus epidermidis and Pseudomonas aeruginosa. Crystal violet assay and scanning electron microscopy (SEM) were used to evaluate the effect of extracts on biofilm formation and measurements of the absorbance at 600 nm to assess bacterial growth. Selected extracts were investigated regarding the cytotoxicity by MTT assay using mammal cells and the qualitative phytochemical fingerprint by thin layer chromatography. Harpochilus neesianus Mart. ex Nees. (Acanthaceae) leaves, Apuleia leiocarpa Vogel J. F. Macbr. (Fabaceae), and Poincianella microphylla Mart. ex G. Don L. P. Queiroz (Fabaceae) fruits showed non-biocidal antibiofilm action against S. epidermidis with activities of 69, 52, and 63%, respectively. SEM confirmed that biofilm structure was strongly prevented and that extracts promoted overproduction of the matrix and/or bacterial morphology modification. Poincianella microphylla demonstrated toxicity at 4.0 mg/mL and 2.0 mg/mL, A. leiocarpa presented toxicity only at 4.0 mg/mL, whereas H. neesianus presented the absence of toxicity against Vero cell line. Preliminary phytochemical analysis revealed the presence of flavonoids, terpenoids, steroids, amines, and polyphenols. This work provides a scientific basis which may justify the ethnopharmacological use of the plants herein studied, indicating extracts that possess limited mammal cytotoxicity in vitro and a high potential as a source of antibiofilm drugs prototypes.

  8. Screening of the Antimicrobial Activities of Some Plants Used ...

    African Journals Online (AJOL)

    ... this study, the extracts were shown to be devoid of activity against Aspergillus flavus, A. niger, Trichophyton mentagrophyte and the clinical isolate of Candida albicans. Keywords: antibacterial activity, antifungal activity, Jasminum abyssinicum, Lagenaria siceraria, Solanecio gigas. Ethiopian Pharmaceutical Journal Vol.

  9. 78 FR 38452 - Agency Information Collection (VA Police Officer Pre-Employment Screening Checklist) Activities...

    Science.gov (United States)

    2013-06-26

    ... From the Federal Register Online via the Government Publishing Office DEPARTMENT OF VETERANS AFFAIRS Agency Information Collection (VA Police Officer Pre-Employment Screening Checklist) Activities Under OMB Review AGENCY: Office of Policy, Planning and Preparedness, Department of Veterans Affairs...

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

    International Nuclear Information System (INIS)

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

    2016-01-01

    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. - Highlights: • Dopamine modified alginate bead and fiber promote cell viability and proliferation. • Alginate-dopamine gel promotes osteogenic differentiation of MSCs. • Dopamine reduced nanosilver for anti-infection. • Alginate-dopamine bead and fiber for delivery of mesenchymal stem cells (MSCs)

  11. Cross-sectional associations between maternal parenting styles, physical activity and screen sedentary time in children

    NARCIS (Netherlands)

    Van Der Geest, K. E.; Mérelle, S. Y. M.; Rodenburg, G.; Van De Mheen, D.; Renders, C. M.

    Background Children’s activity level, including physical activity (PA) and screen sedentary time (SST), is influenced by environmental factors in which parents play a critical role. Different types of parenting styles may influence children’s activity level. Inconsistent results were found on the

  12. Cross-sectional associations between maternal parenting styles, physical activity and screen sedentary time in children

    NARCIS (Netherlands)

    Van der Geest, K E; Mérelle, S Y M; Rodenburg, G; Van de Mheen, D; Renders, C M

    2017-01-01

    BACKGROUND: Children's activity level, including physical activity (PA) and screen sedentary time (SST), is influenced by environmental factors in which parents play a critical role. Different types of parenting styles may influence children's activity level. Inconsistent results were found on the

  13. Screening of some Cuban medicinal plants for antimicrobial activity.

    Science.gov (United States)

    Martínez, M J; Betancourt, J; Alonso-González, N; Jauregui, A

    1996-07-05

    The antimicrobial activities of 23 extracts of 12 Cuban plant species reported in traditional medicine were tested. The agar diffusion method was used to assess the activity against four bacteria and one yeast: Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Pseudomonas aeruginosa and Candida albicans. The results, evaluated as the diameter of the inhibition zone of microbial growth, showed that nine extracts were active against Gram-positive bacteria but only two of these proved to be also active against Gram-negative bacteria. None of the extracts inhibited the growth of the yeast. The most susceptible bacterium was Staphylococcus aureus and the best antibacterial activity was shown by Schinus terebenthifolius.

  14. Active Choice and Financial Incentives to Increase Rates of Screening Colonoscopy-A Randomized Controlled Trial.

    Science.gov (United States)

    Mehta, Shivan J; Feingold, Jordyn; Vandertuyn, Matthew; Niewood, Tess; Cox, Catherine; Doubeni, Chyke A; Volpp, Kevin G; Asch, David A

    2017-11-01

    Behavioral economic approaches could increase uptake for colorectal cancer screening. We performed a randomized controlled trial of 2245 employees to determine whether an email containing a phone number for scheduling (control), an email with the active choice to opt in or opt out (active choice), or the active choice email plus a $100 incentive (financial incentive) increased colonoscopy completion within 3 months. Higher proportions of participants in the financial incentive group underwent screening (3.7%) than in the control (1.6%) or active choice groups (1.5%) (P = .01 and P < .01). We found no difference in uptake of screening between the active choice and control groups (P = .88). The $100 conditional incentive modestly but significantly increased colonoscopy use. ClinicalTrials.gov no: NCT02660671. Copyright © 2017 AGA Institute. Published by Elsevier Inc. All rights reserved.

  15. Phytochemical screening and antimicrobial activity of apiary honey ...

    African Journals Online (AJOL)

    Honey produced by honeybee (Apis mellifera) which is used in herbal medicine was examined for its chemical constituents and antimicrobial activity. The phytochemical analysis of honey showed the presence of alkaloids, flavonoids, saponins, steroids, reducing sugar and glycosides. Antimicrobial activity of honey on fresh ...

  16. 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.

  17. Pharmacological screening of Coriandrum sativum Linn. for hepatoprotective activity.

    Science.gov (United States)

    Pandey, A; Bigoniya, P; Raj, V; Patel, K K

    2011-07-01

    Coriandrum sativum (Linn.), a glabrous, aromatic, herbaceous annual plant, is well known for its use in jaundice. Essential oil, flavonoids, fatty acids, and sterols have been isolated from different parts of C. sativum. The plant has a very effective antioxidant profile showing 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity, lipoxygenase inhibition, phospholipid peroxidation inhibition, iron chelating activity, hydroxyl radical scavenging activity, superoxide dismutation, glutathione reduction and antilipid peroxidation due to its high total phenolic content with the presence of constituents like pyrogallol, caffeic acid, glycitin, etc. This study was aimed at investigating the hepatoprotective activity of C. sativum against carbon tetrachloride (CCl4), with estimation of serum serum glutamyl oxaloacetic acid transaminase (SGOT), serum glutamyl pyruvate transaminase (SGPT), alkaine phosphatase (ALP) and bilirubin, and with liver histopathology. Ethanolic extract was found to be rich in alkaloids, phenolic compounds and flavonoids, and high performance liquid chromatography (HPLC) fingerprinting showed the presence of iso-quercetin and quercetin. C. sativum signifies hepatoprotection by reducing the liver weight, activities of SGOT, SGPT, and ALP, and direct bilirubin of CCl(4) intoxicated animals. Administration of C. sativum extract at 300 mg/kg dose resulted in disappearance of fatty deposit, ballooning degeneration and necrosis, indicating antihepatotoxic activity. The results of this study have led to the conclusion that ethanolic extract of C. sativum possesses hepatoprotective activity which may be due to the antioxidant potential of phenolic compounds.

  18. Investigation of the antimicrobial activity of soy peptides by developing a high throughput drug screening assay

    OpenAIRE

    Dhayakaran, Rekha; Neethirajan, Suresh; Weng, Xuan

    2016-01-01

    Background Antimicrobial resistance is a great concern in the medical community, as well as food industry. Soy peptides were tested against bacterial biofilms for their antimicrobial activity. A high throughput drug screening assay was developed using microfluidic technology, RAMAN spectroscopy, and optical microscopy for rapid screening of antimicrobials and rapid identification of pathogens. Methods Synthesized PGTAVFK and IKAFKEATKVDKVVVLWTA soy peptides were tested against Pseudomonas aer...

  19. Phytochemical screening and antibacterial activity of Garcinia kola ...

    African Journals Online (AJOL)

    , Tannin, Saponin, and Cardiac glycoside, Flavonoid, Terpenoid, Phenols, Anthraquinone and Steroid. However, reducing sugar is absent. The antibacterial activity of the extracts against the isolates showed that ethanol extract is more ...

  20. Phytochemical screening and antimicrobial activity of roots of Murraya koenigii (Linn. Spreng. (Rutaceae

    Directory of Open Access Journals (Sweden)

    Manisha Vats

    2011-12-01

    Full Text Available Murraya koenigii, family Rutaceae, commonly known as Curry leaf plant is a highly valued plant for its medicinal value and characteristic aroma. The plant is a rich source of carbazole alkaloids. The petroleum ether, chloroform, ethyl acetate and ethanol extracts of roots of the plant were screened for phytochemical properties and antimicrobial activity for Staphylococcus aureus, Micrococcus luteus, Bacillus subtilis, Escherichia coli, Pseudomonas aeruginosa, Candida albicans and Aspergillus niger. Phytochemical screening showed the presence of carbohydrates, alkaloids, steroids and flavonoids in the root extracts of the plant. The study shows that all the extracts possess remarkable antibacterial activity. Additionally, petroleum ether and chloroform extracts also had antifungal activity.

  1. 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 barrie...

  2. Are school factors and urbanization supportive for being physically active and engaging in less screen-based activities?

    NARCIS (Netherlands)

    Kopcakova, Jaroslava; Dankulincova Veselska, Zuzana; Madarasova Geckova, Andrea; Klein, Daniel; van Dijk, Jitse P; Reijneveld, Sijmen A

    The aim was to assess the association between physical activity and screen-based activities in adolescents and selected school factors and urbanization and whether these associations were modified by degree of urbanization. We obtained data regarding the fifth-ninth grade students from 130 schools

  3. Further screening of Venda medicinal plants for activity against HIV ...

    African Journals Online (AJOL)

    Owner

    2006-03-15

    Mar 15, 2006 ... by an NIH image apparatus. This means none of the fractions inhibited IN activity at the concentrations tested. (Data not shown). 1H and 14C nuclear magnetic resonance data, MS, UV and infrared spectroscopic data revealed that substance X and Y were the known phytosterols friedelin and β-sistosterol, ...

  4. In vitro antioxidant activity and phytochemical screening of methanol ...

    African Journals Online (AJOL)

    Both extracts showed no significant differences (p > 0.05) in their levels of thiobarbituric acid reactive substances (TBARS). The results suggest that D. edulis and F. capensis leaves possess ample antioxidant activity and phytochemical constituents which may play important roles in the pharmaceutical and food industries.

  5. Screening of some Siberian medicinal plants for antimicrobial activity

    Czech Academy of Sciences Publication Activity Database

    Kokoška, L.; Polesný, Z.; Rada, V.; Nepovím, Aleš; Vaněk, Tomáš

    2002-01-01

    Roč. 82, - (2002), s. 51-53 ISSN 0378-8741 R&D Projects: GA ČR GA525/02/0257 Institutional research plan: CEZ:AV0Z4055905 Keywords : antimicrobial activity * medicinal plants Subject RIV: CE - Biochemistry Impact factor: 1.188, year: 2002

  6. Phytochemical Screening and In-vivo Antipyretic Activity of the ...

    African Journals Online (AJOL)

    Erah

    and timber, including its use for the production of match-sticks. [3]. The leaves are used traditionally in inflammation and cutaneous trouble [3,4]. Its leaf extract exhibits significant antifungal activities against ringworm infection while the bark gum contains catechutannic acid [5]. Dar et al [6] isolated antioxidant and analgesic ...

  7. Screening for Anticandidal and Antibiofilm Activity of Some Herbs in ...

    African Journals Online (AJOL)

    The result of GC-MS analysis showed the major compound of P. betle extract responsible for anticandidal activity as 4-chromanol. Conclusion: P. betle extract contains 4-chromanol which is a good potential anticandidal agent for the treatment of oral infectious diseases caused by certain Candida spp. Keywords: Piper betle ...

  8. Screening of the Antidepressant-like Activity of Two Hypericum ...

    African Journals Online (AJOL)

    Eighty percent methanol extract of H. quartinianum and H. revolutum was investigated using learned helplessness models of depression such as tail suspension test (TST), forced swimming tests (FST) and avoidance tests. In addition, locomotor activity was investigated with open field test (OFT). Mice (for TST, avoidance ...

  9. Evaluation of the Diuretic Activity and Phytochemical Screening of ...

    African Journals Online (AJOL)

    Diuretic activity was examined in adult male rats, which were orally administered with aqueous, methanol and ethyl acetate fractions of 80% methanol extract of R. abyssinicus at doses of 250, 500 and 750 mg/kg; furosemide (10 mg/kg) or vehicle. Total urine output and electrolyte content of the urine was computed over 24 ...

  10. In vitro screening for endocrine disruptive activity in selected South ...

    African Journals Online (AJOL)

    Various waterborne anthropogenic contaminants disrupt the endocrine systems of wildlife and humans, targeting reproductive pathways, among others. Very little is known, however, regarding the occurrence of endocrine disruptive activity in South African freshwater ecosystems, and coastal ecosystems have not been ...

  11. Phytochemical Screening and Evaluation of the Diuretic Activity of ...

    African Journals Online (AJOL)

    Cholistan Institute of Desert Studies (CIDS), The. Islamia University of Bahawalpur. A voucher specimen ..... photometry to sodium and potassium determination in biological fluids. J Biol Chem. 1947; 163: 429-435. 19. Jesupillai M, Jasmine S, Palanivelu M. Diuretic activity of leaves of Erythrina indica L. Int J Green Pharm.

  12. Phytochemical Screening and Mosquito Repellent Activity of the ...

    African Journals Online (AJOL)

    MBI

    2014-12-24

    Dec 24, 2014 ... 25% w/v, were tested for repellency against Anopheles gambiae, and the repellent activity was assessed using the human-bait technique. .... (2006) evaluated the repellency effect of essential oils extracted from some plants ... rearing protocol as described by Mullai and. Jebanesan, 2007; Alexander et al., ...

  13. Phytochemical Screening and In-vivo Antipyretic Activity of the ...

    African Journals Online (AJOL)

    Purpose: To investigate the antipyretic activity of the methanol extract of Bombax malabaricum leaves (MEBM) in rats. Methods: Baker's yeast was used to induce fever in Wistar rats which were divided into four groups. The animal groups were thereafter administered MEBM (200 mg/kg), MEBM (400 mg/kg), paracetamol ...

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

    Directory of Open Access Journals (Sweden)

    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. A questionnaire for screening the micronutrient intake of economically active South African adults.

    Science.gov (United States)

    Senekal, Marjanne; Steyn, Nelia P; Nel, Johanna

    2009-11-01

    The aim of the present study was to develop (phase 1) and validate (phase 2) a screening questionnaire to assess the adequacy of micronutrient intake of economically active South African adults. For identification of indicator foods to be included in the screening questionnaire (phase 1), a comprehensive, eighty-six-item, quantified FFQ that reflected the food sources of thirteen selected micronutrients associated with the nutrition-related health status of South Africans was developed and completed by 554 adults of all four major ethnic groups. Resulting dietary data were subjected to stepwise regression analyses to identify indicator foods to be included in the final screening questionnaire. For validation of frequency of intake reporting of specific food items included in the screening questionnaire (phase 2), a sample of sixty-six African and eighty-four white adult volunteers of both genders completed a 7 d record as well as the screening questionnaire. The frequency of intake of specific food items derived from the two methods was then compared using Spearman correlation coefficients. Phase 1 identified thirty indicator foods that formed the basis of the screening questionnaire. In phase 2, significant correlations were found for the total group for twenty-two out of the thirty items in the questionnaire, with correlations being the best for white females and the poorest for African males and females. A screening questionnaire (thirty-item FFQ) that can be used by researchers and health professionals to assess an individual's risk of inadequate micronutrient intake was developed and validated.

  16. Excess screen time in US children: association with family rules and alternative activities.

    Science.gov (United States)

    Gingold, Janet A; Simon, Alan E; Schoendorf, Kenneth C

    2014-01-01

    We describe the association of screen time in excess of American Academy of Pediatrics recommendations (≤2 h/d) with family television-use policies and regular nonscreen activities among US school-aged children. Data from the 2007 National Survey of Children's Health were used. The sum of minutes spent on television, videos, video games, and recreational computer use was calculated for children 6 to 17 years old. Bivariate and multivariate logistic regression models were used to calculate relative odds of exceeding American Academy of Pediatrics guidelines and of heavy screen use (>4 h/d) for varying family media-use policies and frequency of alternative activities (physical activity and family meals). In all, 49% of school-aged children had screen time >2 h/d and 16% had screen time >4 h/d. Lower frequency of family meals, presence of TV in the bedroom, absence of rules about TV viewing, and less physical activity were associated with both >2 and >4 hours per day of screen time.

  17. State-Mandated Nutrition, Physical Activity, and Screen Time Policies in Child Care Centers.

    Science.gov (United States)

    Chang-Martinez, Catherina; Ahmed, Nasar U; Natale, Ruby A; Messiah, Sarah E

    2017-09-01

    The child care center (CCC) environment presents opportunities for healthy weight promotion in preschoolers. Our study examined the current state of CCC adherence to nutrition, physical activity, and screen time legislative regulations and the differences in their adherence by center socioeconomic position (SEP: low, middle, high) in Miami-Dade County. In 34 CCC, we used the Environment and Policy Assessment and Observation tool to evaluate nutrition, physical activity, and screen time practices during 1-school day. Twenty-five of the centers (73.5%) were participants of the Child and Adult Care Food Program. Almost 80% of the centers adhered to serving low-fat/fat-free milk to children older than 2 years. Only 34.5% served vegetables and 75.9% served whole fruits during meals/snacks. Ninety-four percent of the centers had quiet and active play incorporated into their daily routines. All centers adhered to the 2-hour screen time limit for children older than 2 years. Low- and middle-SEP centers fared better in the serving of fruits, vegetables, and low-fat/fat-free milk. The centers averaged 1 hour in outdoor play regardless of SEP. High-SEP centers had no TV or screen time during day of observation. CCC practices highlight opportunities for improvement in nutrition, physical activity, and screen time practices in the prevention of overweight in early childhood.

  18. Preliminary Screening of a Classical Ayurvedic Formulation for Anticonvulsant Activity

    Directory of Open Access Journals (Sweden)

    Arnab Dhar

    2016-01-01

    Full Text Available Background: Epilepsy is a serious and complex central nervous system disorder associated with recurrent episodes of convulsive seizures due to the imbalance between excitatory (glutamatergic and inhibitory (GABAergic neurotransmitters level in the brain. The available treatments are neither competent to control the seizures nor prevent progress of disease. Since ages, Herbal medicines have remained important sources of medicines in many parts of world which is evidenced through their uses in traditional systems of medicine i.e. Ayurveda, Siddha, Unani, Homeopathy and Chinese etc. Aim: A polyherbal formulation (containing Terminalia chebula Retz., Asparagus racemosus Willd., Embelia ribes Burm. F, Acorus calamus L., Tinospora cordifolia (Willd. Miers, Convolvulus pluricaulis Choisy, Saussurea lappa C.B.Clarke, Achyranthes aspera L. is mentioned in Ayurvedic classics Bhaiṣajya Ratnāvali. The aim of the study was to evaluate the anticonvulsant activity of the formulation in Maximum electroshock and Pentylenetetrazole induced convulsions in rats. Materials and Methods: In the present study, a polyherbal formulation was developed as directed by classical text and evaluated for the anticonvulsant activity using Maximal Electroshock Shock (MES and Pentylenetetrazole (PTZ induced convulsions in rats. Statistical comparison was done by one way ANOVA followed by the Tukey's multiple comparison test. Results: The obtained results showed that the PHF had a protective role on epilepsy. Treatment with PHF significantly improves antioxidant enzymes activities of superoxide dismutase (SOD and glutathione (GSH levels significantly as compared to controls. PHF also significantly decreased malonaldialdehyde (MDA levels in the brain. Moreover, it also attenuated the PTZ-induced increase in the activity of GABA-T in the rat brain. Conclusion: These findings suggest that PHF might have possible efficacy in the treatment of epilepsy.

  19. Preliminary Screening of a Classical Ayurvedic Formulation for Anticonvulsant Activity.

    Science.gov (United States)

    Dhar, Arnab; Maurya, Santosh Kumar; Mishra, Ashish; Singh, Gireesh Kumar; Singh, Manoj Kumar; Seth, Ankit

    2016-01-01

    Epilepsy is a serious and complex central nervous system disorder associated with recurrent episodes of convulsive seizures due to the imbalance between excitatory (glutamatergic) and inhibitory (GABAergic) neurotransmitters level in the brain. The available treatments are neither competent to control the seizures nor prevent progress of disease. Since ages, Herbal medicines have remained important sources of medicines in many parts of world which is evidenced through their uses in traditional systems of medicine i.e. Ayurveda, Siddha, Unani, Homeopathy and Chinese etc. A polyherbal formulation (containing Terminalia chebula Retz., Asparagus racemosus Willd., Embelia ribes Burm. F, Acorus calamus L., Tinospora cordifolia (Willd.) Miers, Convolvulus pluricaulis Choisy, Saussurea lappa C.B.Clarke, Achyranthes aspera L.) is mentioned in Ayurvedic classics Bhaiṣajya Ratnāvali . The aim of the study was to evaluate the anticonvulsant activity of the formulation in Maximum electroshock and Pentylenetetrazole induced convulsions in rats. In the present study, a polyherbal formulation was developed as directed by classical text and evaluated for the anticonvulsant activity using Maximal Electroshock Shock (MES) and Pentylenetetrazole (PTZ) induced convulsions in rats. Statistical comparison was done by one way ANOVA followed by the Tukey's multiple comparison test. The obtained results showed that the PHF had a protective role on epilepsy. Treatment with PHF significantly improves antioxidant enzymes activities of superoxide dismutase (SOD) and glutathione (GSH) levels significantly as compared to controls. PHF also significantly decreased malonaldialdehyde (MDA) levels in the brain. Moreover, it also attenuated the PTZ-induced increase in the activity of GABA-T in the rat brain. These findings suggest that PHF might have possible efficacy in the treatment of epilepsy.

  20. Chitinolytic enzymes from Clostridium aminovalericum: activity screening and purification.

    Science.gov (United States)

    Simůnek, J; Tishchenko, G; Rozhetsky, K; Bartonová, H; Kopecný, J; Hodrová, B

    2004-01-01

    A strain isolated from the feces of takin was identified as Clostridium aminovalericum. In response to various types of chitin used as growth substrates, the bacterium produced a complete array of chitinolytic enzymes: chitinase ('endochitinase'), exochitinase, beta-N-acetylglucosaminidase, chitosanase and chitin deacetylase. The highest activities of chitinase (536 pkat/mL) and exochitinase (747 pkat/mL) were induced by colloidal chitin. Fungal chitin also induced high levels of these enzymes (463 pkat/mL and 502 pkat/mL, respectively). Crab shell chitin was the best inducer of chitosanase activity (232 pkat/mL). The chitinolytic enzymes of this strain were separated from culture filtrate by ion-exchange chromatography on the carboxylic sorbent Polygran 27. At pH 4.5, some isoforms of the chitinolytic enzymes (30% of total enzyme activity) did not bind to Polygran 27. The enzymes were eluted under a stepwise pH gradient (pH 5-8) in 0.1 mol/L phosphate buffer. At merely acidic pH (4.5-5.5), the adsorbed enzymes were co-eluted. However, at pH close to neutral values, the peaks of highly purified isoforms of exochitinases and chitinases were isolated. The protein and enzyme recovery reached 90%.

  1. Screening for antibacterial and antibiofilm activities in Astragalus angulosus

    Directory of Open Access Journals (Sweden)

    Hussein Kanaan

    2017-03-01

    Methods: the plant was collected in April of 2013 and it was divided into several different portions, then its extracts were obtained by maceration using two different solvents. Extract analysis followed directly, where microtiter broth dilution method was employed to assess antibacterial activity, while antibiofilm potential was tested using colorimetric method. Results: whole plant ethanolic extract showed the highest bacteriostatic effect at a concentration of 12.78 mg ml-1 and also was the most versatile exerting its effect against 3 different strains. Other extracts also exhibited an effect but at higher concentrations and each against a single strain. Regarding antibiofilm activity, the majority of the extracts were able to eradicate >50% of Staphylococcus epidermidis preformed biofilm, where the highest activity was obtained with flower fraction extracted in water, achieving 67.7% biofilm eradication at 0.2 mg ml-1. Conclusions: This plant possesses a promising potential in regard to eradicating bacteria and their biofilms, and it is the first contributing step of establishing a library for the endemic Lebanese plants in this domain. [J Complement Med Res 2017; 6(1.000: 50-57

  2. SCREENING OF PLANT EXTRACTS FOR ANTIMICROBIAL ACTIVITY AGAINST BACTERIA

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    Alexander Vatľák

    2014-02-01

    Full Text Available The aim of this study was antimicrobial action of the methanolic extracts of Equisetum arvense L. and Urtica dioica L. against gramnegative and grampositive bacteria. The antimicrobial activities of the extracts against gramnegative bacteria: Escherichia coli CCM 3988, Listeria ivanovii CCM 5884, Listeria innocua CCM 4030, Pseudomonas aeruginosa CCM 1960, Serratia rubidaea CCM 4684 and grampositive bacteria: Brochothrix thermosphacta CCM 4769, Enterococcus raffinosus CCM 4216, Lactobacillus rhamnosus CCM 1828, Paenobacillus larvae CCM 4483 and Staphylococcus epidermis CCM 4418 were determined by the disc diffusion method and the microbroth dilution method according to CLSI. Probit analysis was used in this experiment. Of the 2 plant extracts tested, all extracts showed antimicrobial activity against one or more species of microorganisms. The most antimicrobial activity showed methanolic plant extract of E. arvense against S. epidermis with disc diffusion method and with microbroth dilution method against S. rubidaea and plant extract Urtica dioica with disc diffusion method against P. aeruginosa and with microbroth dilution method against S. rubidaea and E. coli.

  3. 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.

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

    Science.gov (United States)

    Zhang, Yinan; An, Mingqiang

    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.

  5. Reconceptualizing the Link Between Screen Time When Gaming with Physical Activity and Sedentary Behavior.

    Science.gov (United States)

    Kaye, Linda K; Levy, Andrew R

    2017-12-01

    With public health concerns surrounding rates of sedentary behavior (SB), there is often speculation on the role of screen time (in which "computer gaming" is commonly encompassed) as a key contributor to this epidemic. We argue that these assertions are based upon a number of problematic assumptions. Particularly, the notion that screen time necessitates inactivity or SB can be refuted based on the empirical literature. In addition, digital gaming as one so-called problematic screen-time behavior consists of a failed assumption that all games proffer equivalent physical affordances. We argue that these assumptions should be revisited, in which a reconceptualization of screen-time activities (with specific reference to gaming) and its link with inactivity and/or SB should be a key agenda. Within this, we introduce a conceptual model of how this may be realized, with the intention that this may offer a practical guide for researchers, and indeed for health professionals in this field.

  6. Development of a New Decision Tree to Rapidly Screen Chemical Estrogenic Activities of Xenopus laevis.

    Science.gov (United States)

    Wang, Ting; Li, Weiying; Zheng, Xiaofeng; Lin, Zhifen; Kong, Deyang

    2014-02-01

    During the last past decades, there is an increasing number of studies about estrogenic activities of the environmental pollutants on amphibians and many determination methods have been proposed. However, these determination methods are time-consuming and expensive, and a rapid and simple method to screen and test the chemicals for estrogenic activities to amphibians is therefore imperative. Herein is proposed a new decision tree formulated not only with physicochemical parameters but also a biological parameter that was successfully used to screen estrogenic activities of the chemicals on amphibians. The biological parameter, CDOCKER interaction energy (Ebinding ) between chemicals and the target proteins was calculated based on the method of molecular docking, and it was used to revise the decision tree formulated by Hong only with physicochemical parameters for screening estrogenic activity of chemicals in rat. According to the correlation between Ebinding of rat and Xenopus laevis, a new decision tree for estrogenic activities in Xenopus laevis is finally proposed. Then it was validated by using the randomly 8 chemicals which can be frequently exposed to Xenopus laevis, and the agreement between the results from the new decision tree and the ones from experiments is generally satisfactory. Consequently, the new decision tree can be used to screen the estrogenic activities of the chemicals, and combinational use of the Ebinding and classical physicochemical parameters can greatly improves Hong's decision tree. Copyright © 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

  7. Cross-sectional associations between maternal parenting styles, physical activity and screen sedentary time in children

    OpenAIRE

    Van der Geest, K. E.; Mérelle, S. Y. M.; Rodenburg, G.; Van de Mheen, D.; Renders, C. M.

    2017-01-01

    Background Children’s activity level, including physical activity (PA) and screen sedentary time (SST), is influenced by environmental factors in which parents play a critical role. Different types of parenting styles may influence children’s activity level. Inconsistent results were found on the association between parenting styles and PA, and few studies tested the association between parenting styles and SST. This study examined the association between parenting styles, PA and SST and the ...

  8. Drug discovery for Duchenne muscular dystrophy via utrophin promoter activation screening.

    Directory of Open Access Journals (Sweden)

    Catherine Moorwood

    Full Text Available Duchenne muscular dystrophy (DMD is a devastating muscle wasting disease caused by mutations in dystrophin, a muscle cytoskeletal protein. Utrophin is a homologue of dystrophin that can functionally compensate for its absence when expressed at increased levels in the myofibre, as shown by studies in dystrophin-deficient mice. Utrophin upregulation is therefore a promising therapeutic approach for DMD. The use of a small, drug-like molecule to achieve utrophin upregulation offers obvious advantages in terms of delivery and bioavailability. Furthermore, much of the time and expense involved in the development of a new drug can be eliminated by screening molecules that are already approved for clinical use.We developed and validated a cell-based, high-throughput screening assay for utrophin promoter activation, and used it to screen the Prestwick Chemical Library of marketed drugs and natural compounds. Initial screening produced 20 hit molecules, 14 of which exhibited dose-dependent activation of the utrophin promoter and were confirmed as hits. Independent validation demonstrated that one of these compounds, nabumetone, is able to upregulate endogenous utrophin mRNA and protein, in C2C12 muscle cells.We have developed a cell-based, high-throughput screening utrophin promoter assay. Using this assay, we identified and validated a utrophin promoter-activating drug, nabumetone, for which pharmacokinetics and safety in humans are already well described, and which represents a lead compound for utrophin upregulation as a therapy for DMD.

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

    Directory of Open Access Journals (Sweden)

    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.

  10. 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. © 2014 Society for Laboratory Automation and Screening.

  11. CDC Activities for Improving Implementation of Human Papillomavirus Vaccination, Cervical Cancer Screening, and Surveillance Worldwide.

    Science.gov (United States)

    Senkomago, Virginia; Duran, Denise; Loharikar, Anagha; Hyde, Terri B; Markowitz, Lauri E; Unger, Elizabeth R; Saraiya, Mona

    2017-12-01

    Cervical cancer incidence and mortality rates are high, particularly in developing countries. Most cervical cancers can be prevented by human papillomavirus (HPV) vaccination, screening, and timely treatment. The US Centers for Disease Control and Prevention (CDC) provides global technical assistance for implementation and evaluation of HPV vaccination pilot projects and programs and laboratory-related HPV activities to assess HPV vaccines. CDC collaborates with global partners to develop global cervical cancer screening recommendations and manuals, implement screening, create standardized evaluation tools, and provide expertise to monitor outcomes. CDC also trains epidemiologists in cancer prevention through its Field Epidemiology Training Program and is working to improve cancer surveillance by supporting efforts of the World Health Organization in developing cancer registry hubs and assisting countries in estimating costs for developing population-based cancer registries. These activities contribute to the Global Health Security Agenda action packages to improve immunization, surveillance, and the public health workforce globally.

  12. [Screening and identification of Bacillus pumilus producing double active protein of anticoagulation and thrombolysis].

    Science.gov (United States)

    Liu, Binghua; Luo, Yaxiong; Tao, Xuemei; Xie, Xiaoying; Ma, Xupan; Zhang, Lin

    2014-03-04

    The aim of this study was to screen bacteria that can produce antithrombotic. We screened the target bacteria on VY/4 plate and casein plate from more than 20 samples such as water, soil, rabbit manure, sheep manure and deadwood. We detected the antithrombotic activity by fibrin plate and fibrin tube. We identified the target bacteria by morphological characteristics, physical and chemical properties and 16S DNA sequence homology. We obtained 5 strains that can produce antithrombotic. We found that the extracellular protein of strain LDS33 shows both stronger fibrinolytic activity and stronger anticoagulation activity. According to the morphology, physiochemical properties, 16S DNA sequencing and phylogenetic tree, strain LDS33 is identified as Bacillus pumilus. Bacillus pumilus LDS33 can produce highly active anticoagulation and thrombolysis double active protein.

  13. Parental influences on child physical activity and screen viewing time: a population based study

    Directory of Open Access Journals (Sweden)

    Wolfenden Luke

    2010-10-01

    Full Text Available Abstract Background Parents can influence their children's physical activity participation and screen time.This study examined the relative significance of perceived parental barriers and self-efficacy in relation to children's physical activity participation and screen time viewing. The associations between these factors and the behaviours were analysed. Methods Cross-sectional population survey in New South Wales, Australia of parents of pre-school (N = 764, younger (Kindergarten, Grades 2 and 4; N = 1557 and older children (Grades 6, 8 and 10; N = 1665. Parents reported barriers and self-efficacy to influence their child's physical activity and screen time behaviours in a range of circumstances. Differences were examined by child's sex and age group, household income, maternal education and location of residence. The duration of physical activity and screen viewing was measured by parental report for pre-school and younger children and self-report for older children. Associations between parental factors and children's organised, non-organised and total activity and screen time were analysed. Results Cost, lack of opportunities for participation and transport problems were the barriers most often reported, particularly by low income parents and those in rural areas. The number of barriers was inversely related to children's time spent in organised activity, but not their non-organised activity. Higher parental self-efficacy was positively associated with organised physical activity in the younger and older children's groups and the non-organised activity of older children. School-age children (younger and older groups were less likely to meet physical activity guidelines when parents reported ≥4 barriers (OR 3.76, 95% CI 1.25-11.34 and OR 3.72, 95% CI 1.71-8.11 respectively. Low parental self-efficacy was also associated with the likelihood of children exceeding screen time guidelines for each age group (pre-school OR 0.62, 95% CI 0

  14. Young children's screen activities, sweet drink consumption and anthropometry: results from a prospective European study.

    Science.gov (United States)

    Olafsdottir, S; Berg, C; Eiben, G; Lanfer, A; Reisch, L; Ahrens, W; Kourides, Y; Molnár, D; Moreno, L A; Siani, A; Veidebaum, T; Lissner, L

    2014-02-01

    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 (SSB) and increased BMI, BMI z-score and waist to height ratio (WHtR) two years later. A second hypothesis was that SSB consumption mediates the association between the screen activities and changes in the anthropometric measures. The study is a part of the prospective cohort study IDEFICS ("Identification and prevention of dietary and lifestyle-induced health effects in children and infants"), investigating diet, lifestyle and social determinants of obesity in 2 to 9-year-olds in eight European countries (baseline n=16,225, two-year follow-up; n=11,038). Anthropometry was objectively measured, and behaviours were parent-reported. The main hypothesis was supported, but the second hypothesis was not confirmed. The odds ratio of being in the highest quintile of % change in WHtR was 1.26 (95% CI: 1.17-1.36) and in BMI 1.22 (95% CI: 1.13-1.31), for each hour per day watching television. The odds ratio of having increased SSB consumption was 1.19 (95% CI: 1.09-1.29) for each hour per day watching TV. The associations for total screen time were slightly weaker. The results indicate substantial effects of TV viewing and other screen activities for young 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.

  15. Activity, inactivity, and screen time in relation to weight and fatness over adolescence in girls.

    Science.gov (United States)

    Must, Aviva; Bandini, Linda G; Tybor, David J; Phillips, Sarah M; Naumova, Elena N; Dietz, William H

    2007-07-01

    The impact of activity and inactivity on relative weight and fatness change are best evaluated longitudinally. We examined the longitudinal relationship of physical activity, inactivity, and screen time with relative weight status and percentage body fat (%BF) and explored how it differed by parental overweight status. Non-obese pre-menarcheal girls (173), 8 to 12 years old, were followed until 4 years post-menarche. %BF, BMI z-score, and time spent sleeping, sitting, standing, walking, and in vigorous activity were assessed annually. We developed a physical activity index to reflect time and intensity of activity. Inactivity was defined as the sum of time spent sleeping, sitting, and standing. Screen time was defined as time spent viewing television, videotapes, or playing video games. Parental overweight was defined as at least one parent with BMI>25. In separate linear mixed effects models, activity, inactivity, and screen time were unrelated to BMI z-score longitudinally, with and without accounting for parental overweight. After controlling for parental overweight, activity was inversely related (phistory of overweight represent a target population of high priority for interventions around physical activity and inactivity.

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

    Directory of Open Access Journals (Sweden)

    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.

  17. 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.

  18. Early sexual intercourse: Prospective associations with adolescents physical activity and screen time

    NARCIS (Netherlands)

    Avelar e Silva, R.N. (Raquel Nogueira); A.I. Wijtzes (Anne); Van De Bongardt, D. (Daphne); P.M. van de Looij-Jansen (Petra); R. Bannink (Rienke); H. Raat (Hein)

    2016-01-01

    textabstractObjectives: To assess the prospective associations of physical activity behaviors and screen time with early sexual intercourse initiation (i.e., before 15 years) in a large sample of adolescents. Methods: We used two waves of data from the Rotterdam Youth Monitor, a longitudinal study

  19. Early Sexual Intercourse : Prospective Associations with Adolescents Physical Activity and Screen Time

    NARCIS (Netherlands)

    Nogueira Avelar e Silva, R.; Wijtzes, A.; van de Bongardt, D.; van de Looij-Jansen, P.; Bannink, R.; Raat, H.

    2016-01-01

    Objectives: To assess the prospective associations of physical activity behaviors and screen time with early sexual intercourse initiation (i.e., before 15 years) in a large sample of adolescents. Methods: We used two waves of data from the Rotterdam Youth Monitor, a longitudinal study conducted in

  20. 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

  1. 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

  2. A 3-year longitudinal analysis of changes in fitness, physical activity, fatness and screen time

    DEFF Research Database (Denmark)

    Aires, L; Andersen, Lars Bo; Mendonça, D

    2010-01-01

    AIM: To analyse whether changes in physical activity index (PAI), screen time (ST: television, computer) and body mass index (BMI) made a contribution to longitudinal changes in fitness of children and adolescents. Additionally, we analysed the interaction between baseline fitness level and changes...

  3. High-throughput screening for gene libraries expressing carbohydrate hydrolase activity

    NARCIS (Netherlands)

    Leemhuis, Hans; Euverink, Gert-Jan W.; Dijkhuizen, Lubbert

    2003-01-01

    A simple and fast method is described allowing screening of large number of Escherichia coli clones (4000 per day) for the presence of functional or improved carbohydrate hydrolase enzymes. The procedure is relatively cheap and has the advantage that carbohydrate degrading activity can be directly

  4. 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...] Extension of Agency Information Collection Activity Under OMB Review: Certified Cargo Screening Program... Request (ICR), OMB control number 1652-0053, abstracted below to the Office of Management and Budget (OMB...

  5. The nature of the GRE influences the screening for GR-activity enhancing modulators.

    Directory of Open Access Journals (Sweden)

    Karen Dendoncker

    Full Text Available Glucocorticoid resistance (GCR, i.e. unresponsiveness to the beneficial anti-inflammatory activities of the glucocorticoid receptor (GR, poses a serious problem in the treatment of inflammatory diseases. One possible solution to try and overcome GCR, is to identify molecules that prevent or revert GCR by hyper-stimulating the biological activity of the GR. To this purpose, we screened for compounds that potentiate the dexamethasone (Dex-induced transcriptional activity of GR. To monitor GR transcriptional activity, the screen was performed using the lung epithelial cell line A549 in which a glucocorticoid responsive element (GRE coupled to a luciferase reporter gene construct was stably integrated. Histone deacetylase inhibitors (HDACi such as Vorinostat and Belinostat are two broad-spectrum HDACi that strongly increased the Dex-induced luciferase expression in our screening system. In sharp contrast herewith, results from a genome-wide transcriptome analysis of Dex-induced transcripts using RNAseq, revealed that Belinostat impairs the ability of GR to transactivate target genes. The stimulatory effect of Belinostat in the luciferase screen further depends on the nature of the reporter construct. In conclusion, a profound discrepancy was observed between HDACi effects on two different synthetic promoter-luciferase reporter systems. The favorable effect of HDACi on gene expression should be evaluated with care, when considering them as potential therapeutic agents. GEO accession number GSE96649.

  6. 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.

  7. Adolescent physical activity and screen time: associations with the physical home environment

    Directory of Open Access Journals (Sweden)

    Farbakhsh Kian

    2010-11-01

    Full Text Available Abstract Background Previous research on the environment and physical activity has mostly focused on macro-scale environments, such as the neighborhood environment. There has been a paucity of research on the role of micro-scale and proximal environments, such as that of the home which may be particularly relevant for younger adolescents who have more limited independence and mobility. The purpose of this study was to describe associations between the home environment and adolescent physical activity, sedentary time, and screen time. Methods A total of 613 parent-adolescent dyads were included in these analyses from two ongoing cohort studies. Parents completed a Physical Activity and Media Inventory (PAMI of their home environment. Adolescent participants (49% male, 14.5 ± 1.8 years self-reported their participation in screen time behaviors and wore an ActiGraph accelerometer for one week to assess active and sedentary time. Results After adjusting for possible confounders, physical activity equipment density in the home was positively associated with accelerometer-measured physical activity (p Conclusions The home environment was associated with physical activity and screen time behavior in adolescents and differential environmental effects for males and females were observed. Additional research is warranted to more comprehensively assess the home environment and to identify obesogenic typologies of families so that early identification of at-risk families can lead to more informed, targeted intervention efforts.

  8. 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 Louis

    2016-01-01

    BACKGROUND: Reduced ability to activate the medial hamstring muscles during a sports-specific sidecutting movement has been found to be a potential risk factor for non-contact ACL injury. However, whether a reduced ability to activate the medial hamstring muscle is a general neuromuscular...... 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...... football and handball players (16.7±1.3years) participated in the study. Using surface electromyography (EMG) assessment, the neuromuscular activity of medial hamstring muscle (semitendinosus, ST), lateral hamstring muscle (biceps femoris, BF) and quadriceps muscle (vastus lateralis, VL) were monitored...

  9. Anti-infective properties of the melanin-glucan complex obtained from medicinal tinder bracket mushroom, Fomes fomentarius (L.: Fr.) Fr. (Aphyllophoromycetideae).

    Science.gov (United States)

    Seniuk, Olga F; Gorovoj, Leontiy F; Beketova, Galina V; Savichuk, Hatalia O; Rytik, Petr G; Kucherov, Igor I; Prilutskay, Alla B; Prilutsky, Alexandr I

    2011-01-01

    The goal of this investigation was to comparatively study the efficiency of traditionally used anti-infective drugs and biopolymer complexes originated from the medicinal mushroom Fomes fomentarius (L.:Fr.) Fr.: 1) water-soluble melanin-glucan complex (MGC; -80% melanins and -20% beta-glucans) and 2) insoluble chitin-glucan-melanin complex (ChGMC; -70% chitin, -20% beta-glucans, and -10% melanins). Infectious materials (Helicobacter pylori, Candida albicans, and Herpes vulgaris I and HIV-1(zmb) were used in pure cultures of in vitro and in vivo models on experimental animals. Comparison studies of fungal biopolymers and effective modern antifungal, antibacterial, and antiviral drugs were used in in vitro models. The comparative clinical efficiency of ChGMC and of etiotropic pharmaceuticals in models of H. pylori, C. albicans, and H. vulgaris I infection contamination were studied. Using in vitro models, it was established that MGC completely depresses growth of C. albicans. MGC had an antimicrobial effect on H. pylori identical to erythromycin in all concentrations, and had a stronger action on this bacterium than other tested antibiotics. Tested MGC possesses simultaneously weak toxicity and high anti-HIV-1 activity in comparison with zidovudine (Retrovir). The obtained results show that CLUDDT therapy in Wistar rats with the application of ChGMC is, on average, 1.35-1.43 times as effective as a traditional one. Considering the absence of MGC and ChGMC toxic properties on blood cells even in very high concentrations, these complexes may be used as a source of biopolymers for the creation of essentially new agents for wide application in infectious pathology.

  10. Rapid screening for Chlamydia trachomatis infection by detecting ?-mannosidase activity in urogenital tract specimens

    OpenAIRE

    Wang, Ze-yu; Fu, Guang-yu; Wang, Shan-mei; Qin, Dong-chun; Wang, Zhong-quan; Cui, Jing

    2013-01-01

    Abstract Background Chlamydia trachomatis may cause multiple different urogenital tract disorders, but current non-culture assays for rapid screening of C. trachomatis typically use immunochromatography-based methods. We established another new rapid non-culture method for detection of C. trachomatis based on the measurement of α-mannosidase enzymatic activity in urogenital tract specimens. Method To evaluate the performance of this method, α-mannosidase activities of C. trachomatis serotype ...

  11. Dual gene activation and knockout screen reveals directional dependencies in genetic networks. | Office of Cancer Genomics

    Science.gov (United States)

    Understanding the direction of information flow is essential for characterizing how genetic networks affect phenotypes. However, methods to find genetic interactions largely fail to reveal directional dependencies. We combine two orthogonal Cas9 proteins from Streptococcus pyogenes and Staphylococcus aureus to carry out a dual screen in which one gene is activated while a second gene is deleted in the same cell. We analyze the quantitative effects of activation and knockout to calculate genetic interaction and directionality scores for each gene pair.

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

    Directory of Open Access Journals (Sweden)

    Emilda Rosmine

    2016-03-01

    Full Text Available 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 (ER7 and 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 genus Streptomyces. 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.

  13. An improved algorithm for activated protein C resistance and factor V Leiden screening.

    Science.gov (United States)

    Herskovits, Adrianna Z; Morgan, Elizabeth A; Lemire, Susan J; Lindeman, Neal I; Dorfman, David M

    2013-09-01

    To evaluate the performance of a Russell viper venom-based activated protein C resistance (APCR) screening test relative to DNA analysis for the factor V Leiden mutation. We evaluated the concordance between Pefakit APCR screening results and DNA analysis for 435 patients homozygous (n = 11), heterozygous (n = 310), or wild-type (n =114) for the G1691A allele. Using receiver operating characteristic analysis, we found that a cutoff of 1.89 for the APCR ratio yields a sensitivity and specificity of 99.1%. In patients with discrepant genotype-phenotype correlation, their APCR may provide a more clinically relevant result. We compared several strategies for employing reflex testing and found that performing initial APCR screening followed by confirmatory molecular analysis on a subset of cases in the borderline regions between the diagnostic groups can reduce unnecessary testing by approximately 80% without compromising diagnostic accuracy.

  14. Herbal cocktail as anti-infective: promising therapeutic for the treatment of viral diseases.

    Science.gov (United States)

    Marathe, Sandhya A; Datey, Akshay A; Chakravortty, Dipshikha

    2012-08-01

    Herbal products have gained considerable interest among the pharmaceutical companies and consumers due to the minimal side effects associated with them. The bioflavanoids present in these products are the key players in modulating their effects. Several therapeutic effects have been attributed to the bioflavanoids present in green tea and turmeric. Antimicrobial activity is one among the spectrum of activities they exhibit. Curcumin and catechins, the principle components of turmeric and green tea respectively have virucidal and virustatic actions. An antimicrobial composition consisting of extracts from green tea and turmeric have shown to be highly potent against various microbes, especially viruses. In the present review, we have discussed the patents and the antiviral effects of curcumin and catechins. The antimalarial effect of curcumin has also been discussed.

  15. Small cationic antimicrobial peptidomimetics: emerging candidate for the development of potential anti-infective agents.

    Science.gov (United States)

    Lohan, Sandeep; Bisht, Gopal Singh

    2013-01-01

    Rapid increase in the emergence and spread of microbes resistant to conventionally used antibiotics has become a major threat to global health care. Antimicrobial peptides (AMPs) are considered as a potential source of novel antibiotics because of their numerous advantages such as broad-spectrum activity, lower tendency to induce resistance, immunomodulatory response and unique mode of action. However, AMPs have several drawbacks such as; susceptibility to protease degradation, toxicity and high costs of manufacturing. Therefore, extensive research efforts are underway to explore the therapeutic potential of these fascinating natural compounds. This review highlights the potential of small cationic antimicrobial peptidomimetics (SCAMPs; M.W. ≅ 700 Da) as new generation antibiotics. In particular, we focused on recently identified small active pharmacophore from bulky templates of native AMPs, β-peptides, and lipopeptides. In addition, various design strategies recently undertaken to improve the physicochemical properties (proteolytic stability & plasma protein binding) of small cationic peptides have also been discussed.

  16. 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.

  17. Tweaking Innate Immunity: The Promise of Innate Immunologicals as Anti-Infectives

    Directory of Open Access Journals (Sweden)

    Kenneth L Rosenthal

    2006-01-01

    Full Text Available New and exciting insights into the importance of the innate immune system are revolutionizing our understanding of immune defense against infections, pathogenesis, and the treatment and prevention of infectious diseases. The innate immune system uses multiple families of germline-encoded pattern recognition receptors (PRRs to detect infection and trigger a variety of antimicrobial defense mechanisms. PRRs are evolutionarily highly conserved and serve to detect infection by recognizing pathogen-associated molecular patterns that are unique to microorganisms and essential for their survival. Toll-like receptors (TLRs are transmembrane signalling receptors that activate gene expression programs that result in the production of proinflammatory cytokines and chemokines, type I interferons and antimicrobial factors. Furthermore, TLR activation facilitates and guides activation of adaptive immune responses through the activation of dendritic cells. TLRs are localized on the cell surface and in endosomal/lysosomal compartments, where they detect bacterial and viral infections. In contrast, nucleotide-binding oligomerization domain proteins and RNA helicases are located in the cell cytoplasm, where they serve as intracellular PRRs to detect cytoplasmic infections, particularly viruses. Due to their ability to enhance innate immune responses, novel strategies to use ligands, synthetic agonists or antagonists of PRRs (also known as 'innate immunologicals' can be used as stand-alone agents to provide immediate protection or treatment against bacterial, viral or parasitic infections. Furthermore, the newly appreciated importance of innate immunity in initiating and shaping adaptive immune responses is contributing to our understanding of vaccine adjuvants and promises to lead to improved next-generation vaccines.

  18. Epigenetic tailoring for the production of anti-infective cytosporones from the marine fungus Leucostoma persoonii.

    Science.gov (United States)

    Beau, Jeremy; Mahid, Nida; Burda, Whittney N; Harrington, Lacey; Shaw, Lindsey N; Mutka, Tina; Kyle, Dennis E; Barisic, Betty; van Olphen, Alberto; Baker, Bill J

    2012-04-01

    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 IC(90) of 13 µM toward Plasmodium falciparum, with A549 cytotoxicity IC(90) of 437 µM, representing a 90% inhibition therapeutic index (TI(90) = IC(90) A459/IC(90)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).

  19. 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.

  20. Phytochemical screening and in vitro anthelmintic activity of methanol extract of Terminalia citrina leaves

    Directory of Open Access Journals (Sweden)

    Narhari Das

    2015-06-01

    Full Text Available Objective: To evaluate anthelmintic activity of methanolic extract of leaves of Terminalia citrina (T. citrina plant belonging to the Combretaceae family. Methods: The tests of phytochemical screening included alkaloids, flavonoids, tannins, saponins, quinines, anthocyanins, glycosides, carbohydrates and reducing sugars. The anthelmintic activity of methanolic extract of leaves of T. citrina was evaluated against Pheretima posthuma at three different concentrations (25 mg/mL, 50 mg/mL and 100 mg/mL of extracts which involved determination of time of paralysis and time of death of worms. Results: The phytochemical screening of T. citrina leaves revealed the presence of flavonoids, tannins, alkaloids, carbohydrates and reducing sugars. The present study indicated that methanolic extract significantly exhibited paralysis and also caused death of worms especially at highest concentration of 100 mg/mL, as compared to standard reference Albendazole (10 mg/mL. Conclusions: This study suggests that the leaves of T. citrina possess potent anthelmintic activity.

  1. Drug loaded homogeneous electrospun PCL/gelatin hybrid nanofiber structures for anti-infective tissue regeneration membranes.

    Science.gov (United States)

    Xue, Jiajia; He, Min; Liu, Hao; Niu, Yuzhao; Crawford, Aileen; Coates, Phil D; Chen, Dafu; Shi, Rui; Zhang, Liqun

    2014-11-01

    Infection is the major reason for guided tissue regeneration/guided bone regeneration (GTR/GBR) membrane failure in clinical application. In this work, we developed GTR/GBR membranes with localized drug delivery function to prevent infection by electrospinning of poly(ε-caprolactone) (PCL) and gelatin blended with metronidazole (MNA). Acetic acid (HAc) was introduced to improve the miscibility of PCL and gelatin to fabricate homogeneous hybrid nanofiber membranes. The effects of the addition of HAc and the MNA content (0, 1, 5, 10, 20, 30, and 40 wt.% of polymer) on the properties of the membranes were investigated. The membranes showed good mechanical properties, appropriate biodegradation rate and barrier function. The controlled and sustained release of MNA from the membranes significantly prevented the colonization of anaerobic bacteria. Cells could adhere to and proliferate on the membranes without cytotoxicity until the MNA content reached 30%. Subcutaneous implantation in rabbits for 8 months demonstrated that MNA-loaded membranes evoked a less severe inflammatory response depending on the dose of MNA than bare membranes. The biodegradation time of the membranes was appropriate for tissue regeneration. These results indicated the potential for using MNA-loaded PCL/gelatin electrospun membranes as anti-infective GTR/GBR membranes to optimize clinical application of GTR/GBR strategies. Copyright © 2014 Elsevier Ltd. All rights reserved.

  2. Screening for Hypoglycemic Activity on the Leaf Extracts of Nine Medicinal Plants: In-Vivo Evaluation

    Directory of Open Access Journals (Sweden)

    Aditya Arya

    2012-01-01

    Full Text Available The traditional use of certain plants by the tribal community in central India involves using the young leaves for several ailments, including hyperglycaemia; this study was performed to evaluate the effects of the leaf extracts from 9 such plants in the management of diabetes. Initially, hypoglycemic screening was performed on normal rats whose blood glucose levels were measured before and after oral or intraperitoneal (i.p. administration of the extracts at different periods. The plants were screened at doses of 250 mg/kg i.p. or 500 mg/kg orally. Of these, only Centratherum anthelminticum (Asteraceae, Cissus quadrangularis (Vitaceae, and Woodfordia fruticosa Kurz (Lythraceae significantly reduced postprandial blood glucose levels in normal glycemic rats (P < 0.001, with slight reductions effected by Sida acuta Burm F. (P = 0.002 and Parthenium hysterophorus L. (P = 0.017. The extracts that reduced postprandial blood glucose levels both orally and i.p. in the hypoglycemic screening tests were evaluated for glucose challenge in glucose tolerance tests with i.p and oral administration in overnight-fasted normal rats. The results of these tests potentiate the screening data in the management of diabetes mellitus, which requires further studies on the plants that yielded positive results to determine the active compounds in the different plant parts that are responsible for the activity.

  3. Screening of pharmacologically active small molecule compounds identifies antifungal agents against Candida biofilms

    Directory of Open Access Journals (Sweden)

    Takao eWatamoto

    2015-12-01

    Full Text Available Candida species have emerged as important and common opportunistic human pathogens, particularly in immunocompromised individuals. The current antifungal therapies either have toxic side effects or are insufficiently effect. The aim of this study is develop new small-molecule antifungal compounds by library screening methods using C. albicans, and to evaluate their antifungal effects on Candida biofilms and cytotoxic effects on human cells. Wild-type C. albicans strain SC5314 was used in library screening. To identify antifungal compounds, we screened a small-molecule library of 1,280 pharmacologically active compounds (LOPAC1280TM using an antifungal susceptibility test (AST. To investigate the antifungal effects of the hit compounds, ASTs were conducted using Candida strains in various growth modes, including biofilms. We tested the cytotoxicity of the hit compounds using human gingival fibroblast (hGF cells to evaluate their clinical safety. Only 35 compounds were identified by screening, which inhibited the metabolic activity of C. albicans by >50%. Of these, 26 compounds had fungistatic effects and 9 compounds had fungicidal effects on C. albicans. Five compounds, BAY11-7082, BAY11-7085, sanguinarine chloride hydrate, ellipticine and CV-3988, had strong fungicidal effects and could inhibit the metabolic activity of Candida biofilms. However, BAY11-7082, BAY11-7085, sanguinarine chloride hydrate and ellipticine were cytotoxic to hGF cells at low concentrations. CV-3988 showed no cytotoxicity at a fungicidal concentration.Four of the compounds identified, BAY11-7082, BAY11-7085, sanguinarine chloride hydrate and ellipticine, had toxic effects on Candida strains and hGF cells. In contrast, CV-3988 had fungicidal effects on Candida strains, but low cytotoxic effects on hGF cells. Therefore, this screening reveals agent, CV-3988 that was previously unknown to be antifungal agent, which could be a novel therapies for superficial mucosal

  4. Electronic screens in children's bedrooms and adiposity, physical activity and sleep: do the number and type of electronic devices matter?

    Science.gov (United States)

    Chaput, Jean-Philippe; Leduc, Geneviève; Boyer, Charles; Bélanger, Priscilla; LeBlanc, Allana G; Borghese, Michael M; Tremblay, Mark S

    2014-07-11

    To examine whether the number and type of electronic screens available in children's bedrooms matter in their relationship to adiposity, physical activity and sleep. A cross-sectional study was conducted involving 502 children aged 9-11 years from Ottawa, Ontario. The presence (yes/no) of a television (TV), computer or video game system in the child's bedroom was reported by the parents. Percentage body fat was measured using bioelectrical impedance. An accelerometer was worn over seven days to assess moderate-to-vigorous physical activity (MVPA), total sedentary time, sleep duration and sleep efficiency. Screen time was self-reported by the child. After adjustment for age, sex, ethnicity, annual household income and highest level of parental education, children with 2-3 screens in their bedroom had a significantly higher percentage of body fat than children with no screen in their bedroom. However, while children with 2-3 screens in their bedroom engaged in more screen time overall than those with no screen, total sedentary time and MVPA were not significantly different. Sleep duration was not related to the number of screens in the bedroom, but sleep efficiency was significantly lower in children with at least 2 screens in the bedroom. Finally, children having only a TV in their bedroom had significantly higher adiposity than those having no screen at all. In contrast, the presence of a computer in children's bedrooms was not associated with higher adiposity than that of children with no screen. A higher number of screens in a child's bedroom was associated with higher adiposity, more total screen time and lower sleep efficiency. Having a TV in the bedroom appears to be the type of screen presence associated with higher levels of adiposity. Given the popularity of screens among children, these findings are increasingly relevant to health promotion strategies.

  5. Biomedical applications of synthetic, biodegradable polymers for the development of anti-infective strategies.

    Science.gov (United States)

    Bertesteanu, Serban; Chifiriuc, Mariana Carmen; Grumezescu, Alexandru Mihai; Printza, Atnanasia G; Marie-Paule, Thill; Grumezescu, Valentina; Mihaela, Vlad; Lazar, Veronica; Grigore, Raluca

    2014-01-01

    The emergence of antibiotic resistance in microbial strains is representing one of the major threats to public health worldwide, due to the decreased or total cancelling of the available antibiotics effectiveness, correlated with the slow development of novel antibiotics. Due to their excellent biodegradability and biocompatibility, the synthetic polymers could find a lot of biomedical applications, such as the development of biomaterials with optimized properties and of drug delivery systems. This review is focusing on the applications of synthetic, biodegradable polymers for the improvement of antiinfective therapeutic and prophylactic agents (i.e., antimicrobial and anti-inflammatory agents and vaccines) activity, as well as for the design of biomaterials with increased biocompatibility and resistance to microbial colonization.

  6. Maresin 1 Biosynthesis and Proresolving Anti-infective Functions with Human-Localized Aggressive Periodontitis Leukocytes.

    Science.gov (United States)

    Wang, Chin-Wei; Colas, Romain A; Dalli, Jesmond; Arnardottir, Hildur H; Nguyen, Daniel; Hasturk, Hatice; Chiang, Nan; Van Dyke, Thomas E; Serhan, Charles N

    2015-12-14

    Localized aggressive periodontitis (LAP) is a distinct form of early-onset periodontitis linked to periodontal infection with uncontrolled inflammation and leukocyte-mediated tissue destruction. The resolution of inflammation is an active process orchestrated by specialized proresolving lipid mediators (SPMs). Since the level of the Maresin pathway marker 14-hydroxy-docosahexaenoic acid (14-HDHA) was lower in activated peripheral blood from LAP patients, we investigated the Maresin 1 (MaR1) biosynthetic pathway in these subjects and its role in regulating phagocyte functions. Macrophages from LAP patients had a lower level of expression of 12-lipoxygenase (∼30%) and reduced MaR1 (LAP versus healthy controls [HC], 87.8 ± 50 pg/10(6) cells versus 239.1 ± 32 pg/10(6) cells). Phagocytosis by LAP macrophages was reduced ∼40% compared to that of HC, and killing of periodontal pathogens, including Porphyromonas gingivalis and Aggregatibacter actinomycetemcomitans, were similarly reduced. LAP neutrophils also displayed slower kinetics (∼30%) and decreased maximal phagocytosis (∼20% lower) with these pathogens than those of HC. The administration of MaR1 at 1 nM enhanced phagocytosis (31 to 65% increase), intracellular antimicrobial reactive oxygen species production (26 to 71% increase), bacterial killing of these periodontal pathogens (22 to 38% reduction of bacterial titers), and restored impairment of LAP phagocytes. Together, these results suggest that therapeutics targeting the Maresin pathway have clinical utility in treating LAP and other oral diseases associated with infection, inflammation, and altered phagocyte functions. Copyright © 2016, American Society for Microbiology. All Rights Reserved.

  7. A Clinical Drug Library Screen Identifies Tosufloxacin as Being Highly Active against Staphylococcus aureus Persisters

    Directory of Open Access Journals (Sweden)

    Hongxia Niu

    2015-07-01

    Full Text Available To identify effective compounds that are active against Staphylococcus aureus (S. aureus persisters, we screened a clinical drug library consisting of 1524 compounds and identified six drug candidates that had anti-persister activity: tosufloxacin, clinafloxacin, sarafloxacin, doxycycline, thiostrepton, and chlorosalicylanilide. Among them, tosufloxacin had the highest anti-persister activity, which could completely eradicate S. aureus persisters within 2 days in vitro. Clinafloxacin ranked the second with very few persisters surviving the drug exposure. Interestingly, we found that both tosufloxacin and trovafloxacin that had high activity against persisters contained at the N-1 position the 2,4-difluorophenyl group, which is absent in other less active quinolones and may be associated with the high anti-persister activity. Further studies are needed to evaluate tosufloxacin in animal models and to explain its unique activity against bacterial persisters. Our findings may have implications for improved treatment of persistent bacterial infections.

  8. Estrogenic activity of constituents of underarm deodorants determined by E-Screen assay.

    Science.gov (United States)

    Lange, Claudia; Kuch, Bertram; Metzger, Jörg W

    2014-08-01

    The purpose of this study was to ascertain whether different kinds of underarm deodorants commercially available in Germany might contain substances with estrogenic potential which after use enter the aquatic environment via wastewater. Twenty five deodorants produced by ten different manufacturers in the form of sprays, roll-ons and sticks were investigated using an in vitro-test system (E-Screen assay) for the determination of estrogenic activity based on the human breast cancer cell line MCF-7. Seven out of ten spray deodorant samples showed a quantifiable estrogenic activity. In the case of the sticks and roll-ons it was only one out of six and one out of nine, respectively. The 17β-estradiol equivalent concentrations (EEQs) of the samples ranged from 0.1 ng g(-1) to 9 ng g(-1) deodorant. Spray deodorant samples showed the highest activities in the E-Screen assay compared to the stick and roll-on deodorants. In order to identify substances possibly contributing to the observed biological activity the samples were additionally analyzed by GC/MS. The obtained results of this non-target screening led to the selection of 62 single substances present in the deodorants which for their part were analyzed by E-Screen assay. Eight of these single substances, all of them fragrances, showed estrogenic effects with estradiol equivalence factors (EEFs) similar to parabens, a group of 4-hydroxybenzoic acid esters commonly used as preservatives in personal care products, which are known to have a slight estrogenic effect. Thus, these fragrances are obviously responsible to a substantial degree for the observed estrogenic activity of the deodorants. Copyright © 2014 Elsevier Ltd. All rights reserved.

  9. Impact of Policies on Physical Activity and Screen Time Practices in 50 Child-Care Centers in North Carolina.

    Science.gov (United States)

    Erinosho, Temitope; Hales, Derek; Vaughn, Amber; Mazzucca, Stephanie; Ward, Dianne S

    2016-01-01

    This study assessed physical activity and screen time policies in child-care centers and their associations with physical activity and screen time practices and preschool children's (3-5 years old) physical activity. Data were from 50 child-care centers in North Carolina. Center directors reported on the presence/absence of written policies. Trained research assistants observed physical activity and screen time practices in at least 1 preschool classroom across 3 to 4 days. Children (N = 544) wore accelerometers to provide an objective measure of physical activity. Physical activity and screen time policies varied across centers. Observational data showed 82.7 min/d of active play opportunities were provided to children. Screen time provided did not exceed 30 min/d/child at 98% of centers. Accelerometer data showed children spent 38 min/d in moderate-to-vigorous physical activity and 206 min/d in sedentary activity. Policies about staff supervision of media use were negatively associated with screen time (P < .05). Contrary to expectation, policies about physical activity were associated with less time in physical activity. Clear strategies are needed for translating physical activity policies to practice. Further research is needed to evaluate the quality of physical activity policies, their impact on practice, and ease of operationalization.

  10. 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.

  11. 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.

  12. Enzyme activity screening of thermophilic bacteria isolated from Dusun Tua Hot Spring, Malaysia

    Science.gov (United States)

    Msarah, Marwan; Ibrahim, Izyanti; Aqma, Wan Syaidatul

    2018-04-01

    Thermophilic bacteria have biotechnological importance due to the availability of unique enzymes which are stable in extreme circumstances. The aim of this study includes to isolate thermophilic bacteria from hot spring and screen for important enzyme activities. Water samples from the Dusun Tua Hot Spring were collected and the physiochemical characterisation of water was measured. Eight thermophilic bacteria were isolated and determined to have at least three strong enzyme activity including protease, lipase, amylase, cellulase, pectinase and xylanase. The results showed that HuluC2 displayed all the enzyme activities and can be further studied.

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

    Directory of Open Access Journals (Sweden)

    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.

  14. 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. Copyright © 2016 Elsevier Inc. All rights reserved.

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

    Science.gov (United States)

    Husted, Rasmus S; Bencke, Jesper; Andersen, Lars L; Myklebust, Grethe; Kallemose, Thomas; Lauridsen, Hanne B; Hölmich, Per; Aagaard, Per; Zebis, Mette K

    2016-06-01

    Reduced ability to activate the medial hamstring muscles during a sports-specific sidecutting movement has been found to be a potential risk factor for non-contact ACL injury. However, whether a reduced ability to activate the medial hamstring muscle is a general neuromuscular 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. Sixty-two adolescent female elite football and handball players (16.7±1.3years) participated in the study. Using surface electromyography (EMG) assessment, the neuromuscular activity of medial hamstring muscle (semitendinosus, ST), lateral hamstring muscle (biceps femoris, BF) and quadriceps muscle (vastus lateralis, VL) were monitored during three standardized screening tests - i.e. one-legged horizontal hop (OLH), drop vertical jump (DJ) and sidecutting (SC). Neuromuscular pre-activity was measured in the time interval 10ms prior to initial contact on a force plate. For neuromuscular hamstring muscle pre-activity, correlation analysis (Spearman correlation coefficient) showed low-to-moderate correlations between SC and 1) DJ (rs=0.34-0.36, Phamstring pre-activity share some common variance during the examined tests. However, a lack of strong correlation suggests that we cannot generalize one risk factor during one test to another test. The present data demonstrate that one-legged horizontal hop and drop vertical jump testing that are commonly used in the clinical setting does not resemble the specific neuromuscular activity patterns known to exist during sidecutting, a well known high risk movement for non-contact ACL injury. Copyright © 2016 Elsevier B.V. All rights reserved.

  16. The quest for anti-inflammatory and anti-infective biomaterials in clinical translation

    Directory of Open Access Journals (Sweden)

    May Griffith

    2016-09-01

    Full Text Available 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 multi-functional 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 anti-bacterial 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

  17. Corrosion Behavior of Active Screen Plasma Nitrided 38CrMoAl Steel under Marine Environment

    Science.gov (United States)

    Yang, Li; He, Yongyong; Mao, JunYuan; Zhang, Lei

    2017-10-01

    The 38CrMoAl steels were nitrided at different temperatures for 7 h using active screen plasma discharge. The analysis showed that the thick compound layer composed of ɛ-Fe2-3N and γ‧-Fe4N was formed on the surface. The corrosion behavior was evaluated by measuring the anodic polarization curves in natural sea water (similar 3.5% NaCl solution), and observation of corroded surface were conducted. The electromechanical measurements indicated that the corrosion potential of the nitrided specimens shifted to a nobler value compared to that of untreated specimens. Passive regions were also observed in the polarization curves for all the nitrided specimens. These results indicate that active screen plasma nitriding can enhance the corrosion resistance of the 38CrMoAl steel under marine environment.

  18. Phythochemical screening and anticonvulsant activity of Cymbopogon winterianus Jowitt (Poaceae) leaf essential oil in rodents.

    Science.gov (United States)

    Quintans-Júnior, L J; Souza, T T; Leite, B S; Lessa, N M N; Bonjardim, L R; Santos, M R V; Alves, P B; Blank, A F; Antoniolli, A R

    2008-08-01

    Cymbopogon winterianus (Poaceae) is used for its analgesic, anxiolytic and anticonvulsant properties in Brazilian folk medicine. This report aimed to perform phythochemical screening and to investigate the possible anticonvulsant effects of the essential oil (EO) from fresh leaves of C. winterianus in different models of epilepsy. The phytochemical analysis of EO showed presence of geraniol (40.06%), citronellal (27.44%) and citronellol (10.45%) as the main compounds. A behavioral screening demonstrated that EO (100, 200 and 400mg/kg; ip) caused depressant activity on CNS. When administered concurrently, EO (200 and 400mg/kg, ip) significantly reduced the number of animals that exhibited PTZ- and PIC-induced seizures in 50% of the experimental animals (p<0.05). Additionally, EO (100, 200 and 400mg/kg, ip) significantly increased (p<0.05) the latencies of clonic seizures induced by STR. Our results demonstrated a possible activity anticonvulsant of the EO.

  19. 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.

  20. Screening for active tuberculosis before isoniazid preventive therapy among HIV-infected West African adults.

    Science.gov (United States)

    Moh, R; Badjé, A; N'takpé, J-B; Kouamé, G M; Gabillard, D; Ouassa, T; Ouattara, E; Le Carrou, J; Bohoussou, F; Messou, E; Eholié, S; Anglaret, X; Danel, C

    2017-12-01

    TEMPRANO was a multicentre, open-label trial in which human immunodeficiency virus (HIV) infected adults with high CD4 counts were randomised into early or deferred antiretroviral therapy (ART) arms with or without 6-month isoniazid preventive therapy (IPT) in a setting where the World Health Organization (WHO) recommends IPT in HIV-infected patients. Despite the WHO recommendation, IPT coverage remains low due to fear of the presence of undiagnosed active TB before prescribing IPT, and the related risk of drug resistance. To report the frequency of undiagnosed TB in patients enrolled for IPT and describe the results of a 1-month buffer period to avoid prescribing IPT for active TB cases. Patients were screened using a clinical algorithm and chest X-ray at Day 0 and started on isoniazid at Month 1 if no sign/symptom suggestive of TB appeared between Day 0 and Month 1. Of 1030 patients randomised into IPT arms. 10% never started IPT at Month 1. Of these, 23 had active TB, including 16 with prevalent TB. Among the 927 patients who started IPT, 6 had active TB, including 1 with prevalent TB. Only 1 patient with active TB received IPT due to the 1-month buffer period between Day 0 and IPT initiation. In this study, 1.6% of adults considered free of active TB based on clinical screening at pre-inclusion actually had active TB.

  1. Structuring Health in Colorectal Cancer Screening Conversations: An Analysis of Intersecting Activity Systems

    OpenAIRE

    Canary, Heather; Bullis, Connie; Cummings, Jennifer; Kinney, Anita Y.

    2015-01-01

    This study used structurating activity theory to analyze 21 conversations between genetic counselors and individuals at increased risk for familial colorectal cancer (CRC). The qualitative analysis revealed ways elements of family, primary healthcare, cancer prevention and treatment, and other systems emerged in intervention conversations as shaping CRC screening attitudes and behaviors. Results indicate that family stories, norms, and roles are resources for enacting health practices in fami...

  2. Surface Modification of Ferritic Stainless Steel by Active Screen Plasma Nitriding

    OpenAIRE

    NII, Hiroaki; NISHIMOTO, Akio

    2012-01-01

    Plasma nitriding is a surface modification process with a low environmental impact. Active screen plasma nitriding (ASPN) is one of the new plasma nitriding technologies, and can eliminate problems related to conventional direct current plasma nitriding (DCPN). In this study, ferritic stainless steel SUS430 samples were treated by ASPN to increase their wear resistance without decreasing their corrosion resistance. ASPN was performed in a nitrogen-hydrogen atmosphere with 25%N2 + 75%H2 for 18...

  3. [Antibacterial activity of Porphyra spp. epiphytic bacteria and polyketide synthase I gene screening].

    Science.gov (United States)

    Fang, Wenya; Yang, Rui; Zhu, Peng; Shan, Yuanyuan; Yan, Xiaojun

    2009-02-01

    Based on the antibacterial analysis, we screened Polyketide synthase (PKS I) gene from the epiphytic bacteria of Porphyra spp., in order to obtain the PKS I positive strains and detect the potential connection between the PKS pathway and the antibacterial mechanisms. A total of 31 bacteria with broad-spectrum antibacterial activity were screened by agar-screening methods. The 16S rDNA and the Ketosynthase gene were amplified from the genome DNA of these bacteria, which were cloned into pMD19-T vector for sequencing analysis. Porphyra spp. epiphytic bacteria showed broad-spectrum antibacterial activity. Three PKS I positive epiphytic bacteria were obtained from Wenzhou rotten Porphyra spp. samples which had high antibacterial activity. The BLAST results indicated that the Ketosynthase fragments of PKS I from the strains of WPhG3, WPySwl and WPySw2 shared highest similarity (98%, 99%, 98%) to the strains of Bacillus subtilis subsp. Subtilis str. 168 (NP_389602), Bacillus subtilis (ABR19776) and Aspergillus carbonarius (AAZ99721), respectively. Furthermore, the phylogenetic analysis based on 16S rDNA sequences indicated that they belonged to the genus of Bacillus. The flora of Porphyra spp. epiphytic bacteria was complex, which regulated the phycosphere in many ways. The PKS I pathway might be a performance of antibacterial function of Bacillus from Wenzhou rotten samples.

  4. Virtual screening on natural products for discovering active compounds and target information.

    Science.gov (United States)

    Shen, Jianhua; Xu, Xiaoying; Cheng, Feng; Liu, Hong; Luo, Xiaomin; Shen, Jingkang; Chen, Kaixian; Zhao, Weimin; Shen, Xu; Jiang, Hualiang

    2003-11-01

    Natural products, containing inherently large-scale structural diversity than synthetic compounds, have been the major resources of bioactive agents and will continually play as protagonists for discovering new drugs. However, how to access this diverse chemical space efficiently and effectively is an exciting challenge for medicinal chemists and pharmacologists. While virtual screening, which has shown a great promise in drug discovery, will play an important role in digging out lead (active) compounds from natural products. This review focuses on the strategy of virtual screening based on molecular docking and, with successful examples from our laboratory, illustrates the efficiency of virtual screening in discovering active compounds from natural products. On the other hand, the sequencing of the human genome and numerous pathogen genomes has resulted in an unprecedented opportunity for discovering potential new drug targets. Chemogenomics has appeared as a new technology to initiate target discovery by using active compounds as probes to characterize proteome functions. Natural products are the ideal probes for such research. Binding affinity fingerprint is a powerful chemogenomic descriptor to characterize both small molecules and pharmacologically relevant proteins. Therefore, this review also discusses binding affinity fingerprint strategy for identifying target information from the genomic data by using natural products as the probes.

  5. Fractal analysis of visual search activity for mass detection during mammographic screening.

    Science.gov (United States)

    Alamudun, Folami; Yoon, Hong-Jun; Hudson, Kathleen B; Morin-Ducote, Garnetta; Hammond, Tracy; Tourassi, Georgia D

    2017-03-01

    The objective of this study was to assess the complexity of human visual search activity during mammographic screening using fractal analysis and to investigate its relationship with case and reader characteristics. The study was performed for the task of mammographic screening with simultaneous viewing of four coordinated breast views as typically done in clinical practice. Eye-tracking data and diagnostic decisions collected for 100 mammographic cases (25 normal, 25 benign, 50 malignant) from 10 readers (three board certified radiologists and seven Radiology residents), formed the corpus for this study. The fractal dimension of the readers' visual scanning pattern was computed with the Minkowski-Bouligand box-counting method and used as a measure of gaze complexity. Individual factor and group-based interaction ANOVA analysis was performed to study the association between fractal dimension, case pathology, breast density, and reader experience level. The consistency of the observed trends depending on gaze data representation was also examined. Case pathology, breast density, reader experience level, and individual reader differences are all independent predictors of the complexity of visual scanning pattern when screening for breast cancer. No higher order effects were found to be significant. Fractal characterization of visual search behavior during mammographic screening is dependent on case properties and image reader characteristics. © 2017 American Association of Physicists in Medicine.

  6. 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.

  7. 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

    2008-06-01

    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.

  8. Screening of phytochemicals against protease activated receptor 1 (PAR1), a promising target for cancer.

    Science.gov (United States)

    Kakarala, Kavita Kumari; Jamil, Kaiser

    2015-02-01

    Drug resistance and drug-associated toxicity are the primary causes for withdrawal of many drugs, although patient recovery is satisfactory in many instances. Interestingly, the use of phytochemicals in the treatment of cancer as an alternative to synthetic drugs comes with a host of advantages; minimum side effects, good human absorption and low toxicity to normal cells. Protease activated receptor 1 (PAR1) has been established as a promising target in many diseases including various cancers. Strong evidences suggest its role in metastasis also. There are no natural compounds known to inhibit its activity, so we aimed to identify phytochemicals with antagonist activity against PAR1. We screened phytochemicals from Naturally Occurring Plant-based Anticancer Compound-Activity-Target database (NPACT, http://crdd.osdd.net/raghava/npact/ ) against PAR1 using virtual screening workflow of Schrödinger software. It analyzes pharmaceutically relevant properties using Qikprop and calculates binding energy using Glide at three accuracy levels (high-throughput virtual screening, standard precision and extra precision). Our study led to the identification of phytochemicals, which showed interaction with at least one experimentally determined active site residue of PAR1, showed no violations to Lipinski's rule of five along with predicted high human absorption. Furthermore, structural interaction fingerprint analysis indicated that the residues H255, D256, E260, S344, V257, L258, L262, Y337 and S344 may play an important role in the hydrogen bond interactions of the phytochemicals screened. Of these residues, H255 and L258 residues were experimentally proved to be important for antagonist binding. The residues Y183, L237, L258, L262, F271, L332, L333, Y337, L340, A349, Y350, A352, and Y353 showed maximum hydrophobic interactions with the phytochemicals screened. The results of this work suggest that phytochemicals Reissantins D, 24,25-dihydro-27-desoxywithaferin A, Isoguaiacin

  9. Symptom screening among HIV-infected pregnant women is acceptable and has high negative predictive value for active tuberculosis.

    Science.gov (United States)

    Gupta, Amita; Chandrasekhar, Aditya; Gupte, Nikhil; Patil, Sandesh; Bhosale, Ramesh; Sambarey, Pradeep; Ghorpade, Shivahari; Nayak, Uma; Garda, Laila; Sastry, Jayagowri; Bharadwaj, Renu; Bollinger, Robert C

    2011-11-01

    We evaluated tuberculosis (TB) screening among 799 human immunodeficiency virus (HIV)-infected pregnant women in India. Eleven (1.4%) had active TB. The negative predictive value of screening using cough, fever, night sweats, or weight loss was 99.3%. Tuberculin skin test and targeted chest radiography provided no substantial benefit. TB symptom screening, as recommended by the World Health Organization, is effective for ruling out TB in HIV-infected pregnant women.

  10. Screening of Potential Free Radicals Scavenger and Antibacterial Activities of Purwoceng (Pimpinella alpinaMolk).

    Science.gov (United States)

    Wahyuningrum, Retno; Utami, Pri Iswati; Dhiani, Binar Asrining; Kumalasari, Malikhah; Kusumawardani, Rizka Sari

    2016-11-01

    Purwoceng ( Pimpinella alpina Molk) is a traditional medicinal plant used for its aphrodisiac values. This plant was originated Dieng Plateu, Central Java, Indonesia. Purwoceng has been reported to contain steroid, flavonoids, glycoside, saponins, tannins, and phenolic. Based on secondary metabolite compounds of Purwoceng herbs, a research need to be done to determine the other potential free radicals scavenger and antibacterial activities of Purwoceng. The objectives of this research are to screen the potential free radicals scavenger activity of in vitro using DPPH (1,1 diphenyl-2-picryl-hydrazil) radicals and NO• (nitric oxide) radicals, and antibacterial activity of Purwoceng. The extraction is done by a maceration method with petroleum ether, ethyl acetate, and ethanol solvent, respectively. Free radicals scavenger test was performed using DPPH radicals and NO• radicals, while antibacterial activity screening was performed using agar diffusion test. The results showed that ethyl acetate extract of Purwoceng has free radical scavenger activity with IC50 53.07 ppm lower than butylated hydroxytoluene. Ethyl acetate extract and ethanol extract of Purwoceng have antibacterial activity against Staphyloccus aureus , Escherichia coli , and MG42 bacterial isolate.

  11. A fully automated on-line preconcentration and liquid chromatography-tandem mass spectrometry method for the analysis of anti-infectives in wastewaters.

    Science.gov (United States)

    Segura, Pedro A; Gagnon, Christian; Sauvé, Sébastien

    2007-12-05

    We developed and validated a novel on-line preconcentration liquid chromatography-tandem mass spectrometry method for the determination of anti-infectives in wastewaters. The presented method preconcentrates 1 mL of sample in a load column using a switching-valve technique. The method was optimized with respect to sample load flow rate, volume of the load column wash and organic solvent content of the load column wash. The sample is cleaned using a 30% organic solvent washing step and then gradually eluted to an analytical column for separation. To compensate for matrix effects, quantitation was performed using standard additions. Confirmation of the presence of the detected compounds was done using a second selective reaction monitoring transition. Method intra-day precision was less than 9% and inter-day precision %R.S.D. varied between 2.5 and 23%. Limits of detection for the selected anti-infective compounds ranged from 13 to 61 ng L(-1). All the target anti-infectives were found in the city of Montréal WWTP effluent in concentrations ranging from 71 to 289 ng L(-1). This automated method eases the rapid quantitation of those trace contaminants using small sample volumes.

  12. Factor screening in a 12 Run Plackett-Burman design assuming four active factors

    OpenAIRE

    Jin, Yingzi

    2016-01-01

    In this thesis we perform factor screening in a non-regular two-level design by reducing the number of possible sets of active factors to a certain number. The 12 Run Plackett-Burman(PB) design with four active factors is mainly concerned. Our proposed method works through picking up the 6 effects with the highest absolute value out of 10 in each projection model. To evaluate this method, we used the same example as was used in Tyssedal and Shahrukh\\cite{tyssedal2016factor} where variable sel...

  13. Pulsed dc discharge in the presence of active screen for nitriding of high carbon steel

    OpenAIRE

    Saeed, Adnan; Khan, Abdul Waheed; Jan, Faiq; Waqar, Muhammad; Abrar, Muhammad; Mujahid, Zaka - Ul - Islam; Hussnain, Ali; Zakaullah, Muhammad

    2014-01-01

    A discharge of nitrogen - hydrogen mixture by 50 Hz pulsed dc in the presence of active screen cage is investigated by optical emission spectroscopy (OES). The aim is to identify the parameters (mixture ratio, filling pressure and current density) that may lead to high concentration of active species (N2, N2+ and N). The maximum concentration in this experiment is found with 40% H2 - 60% N2, at filling pressure of 3 mbar with current density of 5 mAcm-2. High carbon steel samples are nitrided...

  14. Children, youth, and parents: screening for obesity risk with the spectrum of physical activity.

    Science.gov (United States)

    Gable, Sara; Tosh, Aneesh K

    2014-01-01

    The current article reviews several practical approaches to screening for obesity risk among children and youth, with an emphasis on the spectrum of physical activity. We encourage physicians to utilize evidence-based strategies (e.g., 5-2-1-0), implement motivational interviewing techniques, and focus on "crunch time" (i.e., the period of day after school and before bedtime) when gathering information about physical activity type and intensity. The insights gained are useful for evaluating obesity risk and establishing goals for lifestyle interventions. Characteristics of successful interventions with youth are also discussed and include goal-setting, self-monitoring, and pedometers.

  15. Phytochemical screening, total phenolic content and antioxidant activity of Byrsonima species.

    Science.gov (United States)

    Pereira, V V; Borel, C R; Silva, R R

    2015-01-01

    The species of the Byrsonima genus (Malpighiaceae) have been used in folk medicine to treat gastrointestinal disorders, asthma and skin infections. In this study, the total phenolic content, antioxidant activity and phytochemical screening were carried out in polar extracts of Byrsonima coccolobifolia, Byrsonima verbascifolia and Byrsonima intermedia. The presence of tannins and flavonoids in the samples and high phenols content was observed. B. coccolobifolia and B. intermedia species showed the best results of antioxidant action. It was analysed the correlation between the methods, and there was a great correlation between phenolic content and antioxidant assay, showing that the phenolic substances contribute to the antioxidant activities of these plants.

  16. Biological screening of 100 plant extracts for cosmetic use (II): anti-oxidative activity and free radical scavenging activity.

    Science.gov (United States)

    Kim, B J; Kim, J H; Kim, H P; Heo, M Y

    1997-12-01

    Methanol aqueous extracts of 100 plants were screened for anti-oxidative activity using Fenton's reagent/ethyl linoleate system and for free radical scavenging activity using the 1,1-diphenyl-2-picryl hydrazyl free radical generating system. The results suggest that 14 plants - Alpinia officinarum, Areca catechu, Brassica alba, Cannabis sativa, Curcuma longa, Curcuma aromatica, Eugenia caryophyllata, Evodia officinalis, Paeonia suffruticosa, Rhaphanus sativus, Rheum palmatum, Rhus verniciflua, Trapa bispinosa, Zanthoxylum piperitum - may be potential sources of anti-oxidants. Eight plants - Citrus aurantium, Cornus officinalis, Gleditsia japonica, Lindera strychnifolia, Phragmites communis, Prunus mume, Schizandra chinensis, Terminalia chebula - may be the potential source of free radical scavengers from natural plant.

  17. Proximate composition, phytochemical screening, GC-MS studies of biologically active cannabinoids and antimicrobial activities of Cannabis indica

    Directory of Open Access Journals (Sweden)

    Muhammad Saqib Isahq

    2015-11-01

    Full Text Available Objective: To investigate the proximate composition, minerals analysis, phytochemical screening, gas chromatography-mass spectrometry (GC-MS studies of active cannabinoids and antimicrobial activities of Cannabis indica (C. indica leaves, stems, and seeds. Methods: Standard qualitative protocols of phytochemical screening were accomplished for the identification of biologically active phytochemicals. Minerals in plant samples were analyzed by using atomic absorption spectrophotometer. The resins of C. indica were analyzed for medicinally active cannabinoid compounds by GC-MS. The sample for GC-MS study was mixed with small quantity of n-hexane and 30 mL of acetonitrile solution for the identification of cannabinoids. Agar well diffusion method was used for antibacterial activity. For antifungal activity, the tested fungal strains were sub-cultured on Sabouraud’s dextrose agar at 28 °C. Results: Mineral analysis revealed the presence of sodium, potassium, magnesium and some other minerals in all parts of C. indica. Phytochemical investigation showed the presence of alkaloids, saponins, tannins, flavonoids, sterols and terpenoids. C. indica divulged wide spectrum of antibacterial activities against Staphylococcus aureus, Bacillus cereus, Klebsiella pneumoniae, and Proteus mirabilis. The extracts of plant leaves, seeds and stems showed significant antifungal activities against Aspergillus niger, Aspergillus parasiticus, and Aspergillus oryzae. The biologically active cannabinoids of delta-9-tetrahydrocannabinol (25.040% and cannabidiol (resorcinol, 2-p-mentha-1,8-dien-4-yl-5-pentyl (50.077% were found in Cannabis resin in high percentage. Conclusions: The findings of the study suggested that the existence of biologically active remedial cannabinoids in elevated concentrations and antimicrobial bioassays of C. indica make it a treasured source to be used in herbal preparation for various ailments.

  18. Report - Screening of the Anti-hyperglycemic activity of some medicinal plants of Jordan.

    Science.gov (United States)

    Alkofahi, Ahmad S; Abdul-Razzak, Khalid K; Alzoubi, Karem H; Khabour, Omar F

    2017-05-01

    Diabetes represents a group of common diseases that are characterized by dysregulation of blood glucose levels. Plants are traditionally used for management of diseases including diabetes. In this study, we screened the anti-diabetic effect of extracts of 21 plants grown in Jordan. Extracts of plants were screened for their antihyperglycemic activity. Diabetes was induced in Sprague Dawley rats using Alloxan. Plant extracts were dosed at 1gm/kg. Blood glucose was measured at baseline and at every hour for 3 hours. Results showed that five plants out of the 21 screened showed antihyperglycemic activity. These plants are Phoenix dactylifera L., Tecoma stans (L.) Kunth, Cichorium pumilum Jacq., Phaseolus vulgaris L., and Teucrium polium L. On the other hand, Sarcopoterium spinosum (L.) Spach. and Brassica oleracea L. var. capitata significantly increased blood glucose levels in diabetic rats. The following plant extracts showed neutral effect on blood glucose levels: Plantago major L., Taraxacum cyprium H. Lindb, Artemisia inculta Delile, Marrubium vulgare L., Inula viscosa (L.) Ai, Rubus sanguineus Friv, Coriandrum sativum L., Cucurbita pepo var ovefera, Cucumis sativus L., Hordeum vulgare L., Apium graveolens L., Avena sativa L., Helianthus annus L., and Anethum graveolens L. In conclusion, Jordanian medicinal plants might be useful for managements of blood glucose levels in patients with diabetes.

  19. Rapid screening for Chlamydia trachomatis infection by detecting α-mannosidase activity in urogenital tract specimens.

    Science.gov (United States)

    Wang, Ze-yu; Fu, Guang-yu; Wang, Shan-mei; Qin, Dong-chun; Wang, Zhong-quan; Cui, Jing

    2013-01-24

    Chlamydia trachomatis may cause multiple different urogenital tract disorders, but current non-culture assays for rapid screening of C. trachomatis typically use immunochromatography-based methods. We established another new rapid non-culture method for detection of C. trachomatis based on the measurement of α-mannosidase enzymatic activity in urogenital tract specimens. To evaluate the performance of this method, α-mannosidase activities of C. trachomatis serotype D strain 、 and 29 standard strains related to clinical urogenital pathogens were investigated. Furthermore, 553 urogenital tract specimens were used for clinical assays via cell culture method and ligase chain reaction method (LCR), adopting an expanded gold standard. Only C. trachomatis was positive for α-mannosidase activity among different types of microbes tested in the research. When prostate fluid specimens, which have some interfering activity, were excluded, the sensitivity and specificity of the enzymatic method were 91.8% (78/85) and 98.3% (409/416), respectively. There were no significant differences (P > 0.05). These results showed that α-mannosidase activity could be utilised as a screening marker of C. trachomatis infection.

  20. Rapid screening for Chlamydia trachomatis infection by detecting α-mannosidase activity in urogenital tract specimens

    Directory of Open Access Journals (Sweden)

    Wang Ze-yu

    2013-01-01

    Full Text Available Abstract Background Chlamydia trachomatis may cause multiple different urogenital tract disorders, but current non-culture assays for rapid screening of C. trachomatis typically use immunochromatography-based methods. We established another new rapid non-culture method for detection of C. trachomatis based on the measurement of α-mannosidase enzymatic activity in urogenital tract specimens. Method To evaluate the performance of this method, α-mannosidase activities of C. trachomatis serotype D strain 、 and 29 standard strains related to clinical urogenital pathogens were investigated. Furthermore, 553 urogenital tract specimens were used for clinical assays via cell culture method and ligase chain reaction method (LCR, adopting an expanded gold standard. Results Only C. trachomatis was positive for α-mannosidase activity among different types of microbes tested in the research. When prostate fluid specimens, which have some interfering activity, were excluded, the sensitivity and specificity of the enzymatic method were 91.8% (78/85 and 98.3% (409/416, respectively. There were no significant differences (P > 0.05. Conclusions These results showed that α-mannosidase activity could be utilised as a screening marker of C. trachomatis infection.

  1. A bacteriophage system for screening and study of biologically active polycyclic aromatic hydrocarbons and related compounds.

    Science.gov (United States)

    Hsu, W T; Harvey, R G; Lin, E J; Weiss, S B

    1977-01-01

    The usefulness of bacterial viruses for detecting substances that are potentially carcinogenic is reexamined as a model system for screening biologically active polycyclic aromatic hydrocarbons. A modification of the original assay procedure allows one to distinguish between aromatics that can modify the biological activity of infectious nucleic acids directly and those polycyclic aromatic hydrocarbons that require metabolic activation by Escherichia coli enzymes. The effect of chemical modification of several different polycyclic aromatic hydrocarbons, with respect to their biological activity in the phage assay system, is described. Among the 31 different compounds examined, (+/-)-anti-benzo[a]pyrene-7,8-diol-9,10-epoxide was the most potent inhibitor of infectious phage nucleic acid. The (+) and (-) isomers of the above racemic mixture did not differ significantly in their capacity to inhibit phage replication. PMID:323848

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

    Science.gov (United States)

    Pochapski, Márcia Thaís; Fosquiera, Eliana Cristina; Esmerino, Luís Antônio; dos Santos, Elizabete Brasil; Farago, Paulo Vitor; Santos, Fábio André; Groppo, Francisco Carlos

    2011-01-01

    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. PMID:21716926

  3. Phytochemical screening and antimalarial activity of some plants traditionally used in Indonesia

    Directory of Open Access Journals (Sweden)

    Syamsudin Abdillah

    2015-06-01

    Full Text Available Objective: To evaluate ethanolic extracts of phytochemical screening, in vitro and in vivo antiplasmodial activities of 15 plants used as antimalarial in Sei Kepayang, North Sumatra. Methods: Extraction was done through maceration with 70% ethanol and screened against chemical content, in vitro test anti-plasmodium against Plasmodium falciparum 3D7 strain and in vivo test in mice infected Plasmodium berghei. Results: The results showed that the plant extract contained a group of saponins, flavonoids, alkaloids, quinone, sterols, triterpene, tannins and cumarine. However, extract of Momordica charantia, Carica papaya, Garcinia atroviridis, Alstonia scholaris, Smallanthus sonchifolia and Cassia siamea had strong anti-plasmodium activity both in vitro and in vivo. Conclusions: In vitro and in vivo antiplasmodial activities of 15 plants are used as antimalarial in Sei Kepayang, North Sumatra. All the plants have in vitro and in vivo anti-plasmodium activity except Orthosiphon stamineus and Luffa cylindrica (ED50 > 1 000 mg/kg body weight and IC50 > 100 μg/mL, respectively.

  4. Extremely reduced motion in front of screens: investigating real-world physical activity of adolescents by accelerometry and electronic diary.

    Directory of Open Access Journals (Sweden)

    Judith Streb

    Full Text Available This paper reports accelerometer and electronic dairy data on typical daily activities of 139 school students from grade six and nine. Recordings covered a typical school day for each student and lasted on average for 23 h. Screen activities (watching television and using the computer are compared to several other activities performed while sitting (e.g., playing, eating, sitting in school, and doing homework. Body movement was continuously recorded by four accelerometers and transformed into a motion sore. Our results show that extremely low motion scores, as if subjects were freezing, emerge to a greater extent in front of screens compared to other investigated activities. Given the substantial amount of time young people spend in front of screens and the rising obesity epidemic, our data suggest a mechanism for the association of screen time and obesity.

  5. TRPA1 agonist activity of probenecid desensitizes channel responses: consequences for screening.

    Science.gov (United States)

    McClenaghan, Conor; Zeng, Fanning; Verkuyl, Jan Martin

    2012-12-01

    The transient receptor potential channel subtype A member 1 (TRPA1) is a nonselective cation channel widely viewed as having therapeutic potential, particularly for pain-related indications. Realization of this potential will require potent, selective modulators; however, currently the pharmacology of TRPA1 is poorly defined. As TRPA1 is calcium permeable, calcium indicators offer a simple assay format for high-throughput screening. In this report, we show that probenecid, a uricosuric agent used experimentally in screening to increase loading of calcium-sensitive dyes, activates TRPA1. Prolonged probenecid incubation during the dye-loading process reduces agonist potency upon subsequent challenge. When Chinese Hamster Ovary (CHO)-hTRPA1 or STC-1 cells, which endogenously express TRPA1, were dye loaded in the presence of 2 mM probenecid TRPA1, agonists appeared less potent; EC(50) for allyl isothiocyante agonists in CHO-hTRPA1 was increased from 1.5±0.19 to 7.32±1.20 μM (P<0.01). No significant effect on antagonist potency was observed when using the agonist EC(80) concentration determined under the appropriate dye-loading conditions. We suggest an alternative protocol for calcium imaging using another blocker of anion transport, sulfinpyrazone. This blocker significantly augments indicator dye loading and the screening window, but is not a TRPA1 agonist and has no effect on agonist potency.

  6. Pharmacophore modeling improves virtual screening for novel peroxisome proliferator-activated receptor-gamma ligands

    Science.gov (United States)

    Lewis, Stephanie N.; Garcia, Zulma; Hontecillas, Raquel; Bassaganya-Riera, Josep; Bevan, David R.

    2015-05-01

    Peroxisome proliferator-activated receptor-gamma (PPARγ) is a nuclear hormone receptor involved in regulating various metabolic and immune processes. The PPAR family of receptors possesses a large binding cavity that imparts promiscuity of ligand binding not common to other nuclear receptors. This feature increases the challenge of using computational methods to identify PPAR ligands that will dock favorably into a structural model. Utilizing both ligand- and structure-based pharmacophore methods, we sought to improve agonist prediction by grouping ligands according to pharmacophore features, and pairing models derived from these features with receptor structures for docking. For 22 of the 33 receptor structures evaluated we observed an increase in true positive rate (TPR) when screening was restricted to compounds sharing molecular features found in rosiglitazone. A combination of structure models used for docking resulted in a higher TPR (40 %) when compared to docking with a single structure model (marketed drug database verified the predictive ability of the selected structure models. This study highlights the steps necessary to improve screening for PPARγ ligands using multiple structure models, ligand-based pharmacophore data, evaluation of protein-ligand interactions, and comparison of docking datasets. The unique combination of methods presented here holds potential for more efficient screening of compounds with unknown affinity for PPARγ that could serve as candidates for therapeutic development.

  7. Adherence to diabetes guidelines for screening, physical activity and medication and onset of complications and death.

    Science.gov (United States)

    Chen, Yiqun; Sloan, Frank A; Yashkin, Arseniy P

    2015-01-01

    Analyze relationships between adherence to guidelines for diabetes care - regular screening; physical activity; and medication - and diabetes complications and mortality. Outcomes were onset of congestive heart failure (CHF), stroke, renal failure, moderate complications of lower extremities, lower-limb amputation, proliferative diabetic retinopathy (PDR), and mortality during follow-up. Participants were persons aged 65+ in the Health and Retirement Study (HRS) 2003 Diabetes Study and had Medicare claims in follow-up period (2004-8). Adherence to screening recommendations decreased risks of developing CHF (odds ratio (OR)=0.83; 95% confidence interval (CI): 0.72-0.96), stroke (OR=0.80; 95% CI: 0.68-0.94); renal failure (OR=0. 82; 95% CI: 0.71-0.95); and death (OR=0.86; 95% CI: 0.74-0.99). Adherence to physical activity recommendation reduced risks of stroke (OR=0.64; 95% CI: 0.45-0.90), renal failure (OR=0.71; 95% CI: 0.52-0.97), moderate lower-extremity complications (OR=0.71; 95% CI: 0.51-0.99), having a lower limb amputation (OR=0.31, 95% CI: 0.11-0.85), and death (OR=0.56, 95% CI: 0.41-0.77). Medication adherence was associated with lower risks of PDR (OR=0.35, 95% CI: 0.13-0.93). Adherence to screening, physical activity and medication guidelines was associated with lower risks of diabetes complications and death. Relative importance of adherence differed among outcome measures. Copyright © 2015. Published by Elsevier Inc.

  8. Exploring the structure–activity relationships of ABCC2 modulators using a screening approach

    Science.gov (United States)

    Wissel, Gloria; Kudryavtsev, Pavel; Ghemtio, Leo; Tammela, Päivi; Wipf, Peter; Yliperttula, Marjo; Finel, Moshe; Urtti, Arto; Kidron, Heidi; Xhaard, Henri

    2015-01-01

    ABCC2 is a transporter with key influence on liver and kidney pharmacokinetics. In order to explore the structure–activity relationships of compounds that modulate ABCC2, and by doing so gain insights into drug–drug interactions, we screened a library of 432 compounds for modulators of radiolabeled β-estradiol 17-(β-D-glucuronide) (EG) and fluorescent 2′,7′-dichlorofluorescin transport (CDCF) in membrane vesicles. Following the primary screen at 80 μM, dose–response curves were used to investigate in detail 86 compounds, identifying 16 low μM inhibitors and providing data about the structure–activity relationships in four series containing 19, 24, 10, and eight analogues. Measurements with the CDCF probe were consistently more robust than for the EG probe. Only one compound was clearly probe-selective with 50-fold difference in the IC50s obtained by the two assays. We built 24 classification models using the SVM and fused-XY Kohonen methods, revealing molecular descriptors related to number of rings, solubility and lipophilicity as important to distinguish inhibitors from inactive compounds. This study is to our best knowledge the first to provide details about structure–activity relationships in ABCC2 modulation. PMID:25935289

  9. A high-throughput colorimetric screening assay for terpene synthase activity based on substrate consumption.

    Directory of Open Access Journals (Sweden)

    Maiko Furubayashi

    Full Text Available Terpene synthases catalyze the formation of a variety of terpene chemical structures. Systematic mutagenesis studies have been effective in providing insights into the characteristic and complex mechanisms of C-C bond formations and in exploring the enzymatic potential for inventing new chemical structures. In addition, there is growing demand to increase terpene synthase activity in heterologous hosts, given the maturation of metabolic engineering and host breeding for terpenoid synthesis. We have developed a simple screening method for the cellular activities of terpene synthases by scoring their substrate consumption based on the color loss of the cell harboring carotenoid pathways. We demonstrate that this method can be used to detect activities of various terpene synthase or prenyltransferase genes in a high-throughput manner, irrespective of the product type, enabling the mutation analysis and directed evolution of terpene synthases. We also report the possibility for substrate-specific screening system of terpene synthases by taking advantage of the substrate-size specificity of C30 and C40 carotenoid pathways.

  10. 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

  11. In vitro antimicrobial, antioxidant activity and phytochemical screening of Apium graveolens.

    Science.gov (United States)

    Uddin, Zakir; Shad, Anwar Ali; Bakht, Jehan; Ullah, Inam; Jan, Saleem

    2015-09-01

    The present study evaluates the phytochemical screenings, antioxidant activity and antimicrobial assay of Apium graveolens L. The phytochemical screening showed the presence of flavonoids, tannins, saponins and steroids in Apium graveolens while terpenoids was absent. The total phenolic content was slightly higher in methanolic fraction (63.46 ± 12.00 mg GAE/g) followed by ethanol (36.60 ± 12.28 mg GAE/g) and hexane fractions (34.86 ± 6.96 mg GAE/g). The flavonoid content was high in methanolic extract (56.95 ± 7.14 mg Quorcetin/g) and low level of the content was found in methylated spirit extract (29.2 ± 3.15 mg Quercitin/g). Antioxidant activity assayed by FRAP was higher in methanolic fraction (12.48 ± 1.06 mmole of FeSO₄equivalent/litre of extract) compared with other extracts. Likewise, good antimicrobial activity was measured by crude ethanol fraction against S. aureus (MIC=0.12 ± 0.03 μg/ml) and S. typhi (MIC= 0.5 ± 0.2 μg/ml). Results also that ethanolic fraction was effective against A. flavus (MIC= 05 ± 1.0 μg/ml).

  12. In vitro Antimicrobial Activity ofCitrus aurantifolia and its Phytochemical screening

    Directory of Open Access Journals (Sweden)

    Rafi khan Pathan

    2012-05-01

    Full Text Available Objective: To evaluate the antimicrobial efficacy of Citrus aurantifolia Linn (CA against some microorganisms - bacteria and fungus were Staphylococcus aureus, Escherichia coli, Klebsiella pneumonia, Pseudomonas spp, Aspergillus niger, Aspergillus fumigates, Mucor spp and Pencillium. Methods: 100 毺 l of 10 mg CA were assessed against eight test microorganisms by agar well Diffusion Method. Gentamicin and Ketoconazole 10 mg/ml were used as standards. A different solvent was used to obtain CA leaf extract by using maceration technique. Results: %yield obtained for dried leaf extract of CA with chloroform, ethanol, acetone, petroleum ether and aqueous ethanol was approximately 15%, 18%, 09%, 11% and 24% respectively. Due to its high yield value hydroalcoholic extract of CA was used for estimating the antimicrobial activity and its phytochemical screening. Phytochemical screening of CA plant reveals the presence of Alkaloids, carbohydrates, flavonoids, steroids and tannins. Conclusions: The study demonstrates that the hydroalcoholic extract of CA leaf exhibit antibacterial activity on Klebsiella pneumonia, Pseudomonas sp, Staphylococcus aureus and antifungal activity among Aspergillus niger, Aspergillus fumigates, Mucor species. These recognized a good support to the use of this plant in herbal medicine and as base for the development of new drugs and phytomedicine.

  13. Screening for motor coordination challenges in children using teacher ratings of physical ability and activity.

    Science.gov (United States)

    Faught, Brent E; Cairney, John; Hay, John; Veldhuizen, Scott; Missiuna, Cheryl; Spironello, Cristina A

    2008-04-01

    We examined the effectiveness of a teacher-based rating scale called the teacher estimation of activity form (TEAF) to screen for developmental coordination disorder (DCD) in children. A random selection of 15 of 75 schools from the District School Board of Niagara in Ontario, Canada was chosen for this study. Every consented child in Grade 4 (n=502) was evaluated for probable DCD (pDCD) in school using the short form Bruininks-Oseretsky test of motor proficiency (BOTMP-SF). Each student also completed the children's self perceptions of adequacy in and predilection toward physical activity (CSAPPA) scale, participation questionnaire, and Léger 20-meter shuttle run, and had their height and weight measured. The 27 children (5.1%) who scored below the 5th percentile on BOTMP-SF were designated as pDCD cases and the 475 children who scored above the 5th percentile served as controls. Results showed that mean TEAF scores were significantly lower for pDCD children than controls (pphysical activity and fitness. The TEAF appears to be an effective tool in screening for DCD, particularly in a population setting. Considering the brevity of the TEAF and the discriminative power of individual items, this instrument would be effective in an abbreviated version.

  14. Anti-angiogenic activity and phytochemical screening of fruit fractions from Vitex agnus castus.

    Science.gov (United States)

    Certo, Giovanna; Costa, Rosaria; D'Angelo, Valeria; Russo, Marina; Albergamo, Ambrogina; Dugo, Giacomo; Germanò, Maria Paola

    2017-12-01

    Although the antitumour activity of Vitex agnus castus fruits has been already addressed, no work has yet assessed their anti-angiogenic potential. To this purpose, several extractive fractions of such fruits were tested on zebrafish embrios by EAP assay, so that only the bioactive fractions could be subsequently tested on the chick chorioallantoic membrane by CAM assay. Bioactive fractions were also phytochemically screened to identify those bioactive compounds responsible for anti-angiogenic activity. A marked inhibition of vessel formation was detected only in zebrafish embryos treated with chloroform or ethyl acetate fractions. Considering CAM assay, chloroform fraction induced a strong reduction of microvasculature and haemoglobin content; while lower anti-angiogenic effects of the ethyl acetate fraction were determined. Phytochemical analyses confirmed the presence of several bioactive anti-angiogenic compounds. Overall, obtained preliminary results highlighted a potential anti-angiogenic activity of V. agnus castus fruits.

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

    International Nuclear Information System (INIS)

    Yousaf, A.; Latif, Z.

    2014-01-01

    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)

  16. 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

    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......, 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 vitro, indicating the relevance of elucidating the endocrine effects in vivo of these compounds....

  17. Curating and Preparing High-Throughput Screening Data for Quantitative Structure-Activity Relationship Modeling.

    Science.gov (United States)

    Kim, Marlene T; Wang, Wenyi; Sedykh, Alexander; Zhu, Hao

    2016-01-01

    Publicly available bioassay data often contains errors. Curating massive bioassay data, especially high-throughput screening (HTS) data, for Quantitative Structure-Activity Relationship (QSAR) modeling requires the assistance of automated data curation tools. Using automated data curation tools are beneficial to users, especially ones without prior computer skills, because many platforms have been developed and optimized based on standardized requirements. As a result, the users do not need to extensively configure the curation tool prior to the application procedure. In this chapter, a freely available automatic tool to curate and prepare HTS data for QSAR modeling purposes will be described.

  18. 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...

  19. School Term vs. School Holiday: Associations with Children's Physical Activity, Screen-Time, Diet and Sleep.

    Science.gov (United States)

    Staiano, Amanda E; Broyles, Stephanie T; Katzmarzyk, Peter T

    2015-07-30

    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.

  20. 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.

  1. Aqueous zymography screening of matrix metalloproteinase activity and inhibition based on colorimetric gold nanoparticles.

    Science.gov (United States)

    Chuang, Yao-Chen; Huang, Wei-Ting; Chiang, Pin-Hsuan; Tang, Meng-Che; Lin, Chih-Sheng

    2012-02-15

    An optical gold nanoparticles (AuNPs)-based method was fabricated for the rapid detection of matrix metalloproteinase (MMP) activity and screening potential MMP inhibitors without sophisticated instruments. The diagnosis platform was composed of AuNPs, particular MMP substrates and 6-mercapto-1-hexanol (MCH). The functionalized AuNPs were subjected to specific MMP digestion, and the MMP found the substrate on AuNPs, such that the AuNPs lost shelter and MCH increased the attraction force between AuNPs. Consequently, AuNPs aggregation and a color change from red to purple with increasing MMP concentration were observed. The surface plasmon resonance (SPR) of the formed AuNPs allowed for the quantitative detection of MMP activity. A sensitive linear correlation existed between the absorbance and the activity of the MMPs, which ranged from 10 ng/mL to 700 ng/mL in NTTC buffer and plasma samples. The proposed colorimetric method could be accomplished in a homogeneous solution with one-step operation in 30 min and has been successfully applied to the determination of particular MMP activity in plasma samples, in which the results are consistent with substrate zymography. This technology may become a simple platform for parallel screening a number of inhibitors and offer an alternative method to studying the efficiency of inhibitors for suppressing MMP activity. The absorbance ratio at 625 nm and 525 nm (A(625)/A(525)) confirmed the efficiency of the inhibitors as observed in substrate zymography. The IC(50) of ONO-4817 and galardin for MMP-1, MMP-2 and MMP-7 determined by the proposed colorimetric method was similar to the results of substrate zymography. Crown Copyright © 2011. Published by Elsevier B.V. All rights reserved.

  2. Phytochemical screening, total phenolic, total flavonoids contents and antioxidant activity of cinchona ledgeriana leaves ethanol extract

    Science.gov (United States)

    Sundowo, Andini; Artanti, Nina; Hanafi, M.; Minarti, Primahana, Gian

    2017-11-01

    C ledgeriana is a medicinal plant that contains alkaloids, especially on the barks for commercial production of quinine as antimalarial. The main alkaloids in this plant are cinchonine, cinchonidine, quinine and quinidine. Besides for antiamalarial this plant is also commonly used to treat whooping cough, influenza and dysentery. Compare to other medicinal plants, nowadays only very few studies were conducted in Cinchona species. Our current study aims to determine the content of phytochemical, total phenol and total flavonoids from C. ledgeriana leaves 70% ethanol extract. The extraction was performed by maceration method using 70% ethanol solvent and then fractionated into hexane, ethylacetate and butanol. Phytochemical screening was performed to determine the content of alkaloids, flavonoids, terpenoids, tannins and saponins. Total phenol and flavonoid contents of the extract were determined by Folin-Ciocalteu and alumunium chloride colorimetric methods using gallic acid and quercetin as standards. The antioxidant activity was determined by using 2, 2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity. The results of phytochemical screening showed that the 70% ethanol extract of C. ledgeriana leaves contained alkaloids, flavonoids, terpenoids, tannins and saponins. The total phenol and total flavonoids analysis showed that ethyl acetate fraction had the highest total phenol (40.23%) and total flavonoids (65.34%).

  3. Research resource: modulators of glucocorticoid receptor activity identified by a new high-throughput screening assay.

    Science.gov (United States)

    Blackford, John A; Brimacombe, Kyle R; Dougherty, Edward J; Pradhan, Madhumita; Shen, Min; Li, Zhuyin; Auld, Douglas S; Chow, Carson C; Austin, Christopher P; Simons, S Stoney

    2014-07-01

    Glucocorticoid steroids affect almost every type of tissue and thus are widely used to treat a variety of human pathological conditions. However, the severity of numerous side effects limits the frequency and duration of glucocorticoid treatments. Of the numerous approaches to control off-target responses to glucocorticoids, small molecules and pharmaceuticals offer several advantages. Here we describe a new, extended high-throughput screen in intact cells to identify small molecule modulators of dexamethasone-induced glucocorticoid receptor (GR) transcriptional activity. The novelty of this assay is that it monitors changes in both GR maximal activity (A(max)) and EC(50) (the position of the dexamethasone dose-response curve). Upon screening 1280 chemicals, 10 with the greatest changes in the absolute value of A(max) or EC(50) were selected for further examination. Qualitatively identical behaviors for 60% to 90% of the chemicals were observed in a completely different system, suggesting that other systems will be similarly affected by these chemicals. Additional analysis of the 10 chemicals in a recently described competition assay determined their kinetically defined mechanism and site of action. Some chemicals had similar mechanisms of action despite divergent effects on the level of the GR-induced product. These combined assays offer a straightforward method of identifying numerous new pharmaceuticals that can alter GR transactivation in ways that could be clinically useful.

  4. Screening for glycosidase activities of lactic acid bacteria as a biotechnological tool in oenology.

    Science.gov (United States)

    Pérez-Martín, Fátima; Seseña, Susana; Izquierdo, Pedro Miguel; Martín, Raúl; Palop, María Llanos

    2012-04-01

    The aim of this study was to evaluate the ability from a number of lactic acid bacteria isolated from different sources to produce glycosidase enzymes. Representative isolates (225) from clusters obtained after genotyping, using randomly amplified polymorphic DNA-polymerase chain reaction (RAPD-PCR) analysis, of 1,464 isolates, were screened for β-D-glucosidase activity. Thirty-five of them were selected for subsequent analysis. These strains were able to hydrolyze α-D-glucopyranoside, β-D-xylopyranoside and α-L-arabinofuranoside although β-D-glucosidase activity was the predominant activity for 22 of the selected strains. Only some of them did so with α-L-rhamnopyranoside. All of these were from wine samples and were identified as belonging to the Oenococcus oeni species using Amplification and Restriction Analysis of 16S-rRNA gene (16S-ARDRA). When the influence of pH, temperature and ethanol or sugars content on β-D-glucosidase activity was assayed, a strain-dependent response was observed. The β-D-glucosidase activity occurred in both whole and sonicated cells but not in the supernatants from cultures or obtained after cell sonication. Strains 10, 17, 21, and 23 retained the most β-D-glucosidase activity when they were assayed at the conditions of temperature, pH, ethanol and sugar content used in winemaking. These results suggest that these strains could be used as a source of glycosidase enzymes for use in winemaking.

  5. Screening of antimicrobial activity of macroalgae extracts from the Moroccan Atlantic coast.

    Science.gov (United States)

    El Wahidi, M; El Amraoui, B; El Amraoui, M; Bamhaoud, T

    2015-05-01

    The aim of this work is the screening of the antimicrobial activity of seaweed extracts against pathogenic bacteria and yeasts. The antimicrobial activity of the dichloromethane and ethanol extracts of ten marine macroalgae collected from the Moroccan's Atlantic coast (El-Jadida) was tested against two Gram+ (Bacillus subtilis and Staphylococcus aureus) and two Gram- (Escherichia coli and Pseudomonas aeruginosa) human pathogenic bacteria, and against two pathogenic yeasts (Candida albicans and Cryptococcus neoformans) using the agar disk-diffusion method. Seven algae (70%) of ten seaweeds are active against at least one pathogenic microorganisms studied. Five (50%) are active against the two studied yeast with an inhibition diameter greater than 15 mm for Cystoseira brachycarpa. Six (60%) seaweeds are active against at least one studied bacteria with five (50%) algae exhibiting antibacterial inhibition diameter greater than 15 mm. Cystoseira brachycarpa, Cystoseira compressa, Fucus vesiculosus, and Gelidium sesquipedale have a better antimicrobial activity with a broad spectrum antimicrobial and are a potential source of antimicrobial compounds and can be subject of isolation of the natural antimicrobials. Copyright © 2015 Elsevier Masson SAS. All rights reserved.

  6. An opportunity to address modifiable breast cancer risks: Mammography screening and physical activity readiness to change

    Directory of Open Access Journals (Sweden)

    Maria D. Thomson, PhD

    2017-03-01

    Full Text Available Breast cancer risk is significantly reduced by improvements in lifestyle factors such as physical activity. Previous work suggests personal experiences such as false positive mammography or family history of breast cancer may influence these health behaviors. Surveys were distributed to women aged 40–75 who had received a negative mammogram from an academic hospital in Virginia in 2015. Measures assessed breast cancer worry and perceived risk, awareness of cancer risk factors, family history of breast cancer, false positive mammography experience, and readiness to change physical activity. Surveys were collected from 106 women. The regression for readiness to change physical activity was significant, F(7, 91 = 3.7, p = 0.001, R2 = 0.22. Physical activity readiness to change was positively associated with income (p = 0.034 and receipt of a false positive mammogram (p = 0.045. African American women (p = 0.031 and women with family history of breast cancer (p = 0.027 reported lower readiness to change physical activity. Results support previous qualitative work suggesting the receipt of a false positive mammogram may stimulate motivation to increase physical activity. Mammography screening may serve as a strategic opportunity to target modifiable breast cancer risk factors at a time when women are highly receptive to a lifestyle change intervention.

  7. Biosynthesis of silver nanoparticles using Ocimum sanctum (Tulsi) leaf extract and screening its antimicrobial activity

    Science.gov (United States)

    Singhal, Garima; Bhavesh, Riju; Kasariya, Kunal; Sharma, Ashish Ranjan; Singh, Rajendra Pal

    2011-07-01

    Development of green nanotechnology is generating interest of researchers toward ecofriendly biosynthesis of nanoparticles. In this study, biosynthesis of stable silver nanoparticles was done using Tulsi ( Ocimum sanctum) leaf extract. These biosynthesized nanoparticles were characterized with the help of UV-vis spectrophotometer, Atomic Absorption Spectroscopy (AAS), Dynamic light scattering (DLS), X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), and Transmission electron microscopy (TEM). Stability of bioreduced silver nanoparticles was analyzed using UV-vis absorption spectra, and their antimicrobial activity was screened against both gram-negative and gram-positive microorganisms. It was observed that O. sanctum leaf extract can reduce silver ions into silver nanoparticles within 8 min of reaction time. Thus, this method can be used for rapid and ecofriendly biosynthesis of stable silver nanoparticles of size range 4-30 nm possessing antimicrobial activity suggesting their possible application in medical industry.

  8. Analysis of High-Dimensional Structure-Activity Screening Datasets Using the Optimal Bit String Tree.

    Science.gov (United States)

    Zhang, Ke; Hughes-Oliver, Jacqueline M; Young, S Stanley

    2013-01-01

    A new classification method called the Optimal Bit String Tree is proposed to identify quantitative structure-activity relationships (QSARs). The method introduces the concept of a chromosome to describe the presence/absence context of a combination of descriptors. A descriptor set and its optimal chromosome form the splitting variable. A new stochastic searching scheme that contains a weighted sampling scheme, simulated annealing, and a trimming procedure optimizes the choice of splitting variable. Simulation studies and an application to screening monoamine oxidase (MAO) inhibitors show that OBSTree is advantageous in accurately and effectively identifying QSAR rules and finding different classes of active compounds. Details of the algorithm, SAS code, and simulated and real datasets are available online as supplementary materials.

  9. Examining the Relationship Between the Functional Movement Screen and the Landing Error Scoring System in an Active, Male Collegiate Population.

    Science.gov (United States)

    Everard, Eoin M; Harrison, Andrew J; Lyons, Mark

    2017-05-01

    Everard, EM, Harrison, AJ, and Lyons, M. Examining the relationship between the functional movement screen and the landing error scoring system in an active, male collegiate population. J Strength Cond Res 31(5): 1265-1272, 2017-In recent years, there has been an increasing focus on movement screening as the principal aspect of preparticipation testing. Two of the most common movement screening tools are the Functional Movement Screen (FMS) and the Landing Error Scoring System (LESS). Several studies have examined the reliability and validity of these tools, but so far, there have been no studies comparing the results of these 2 screening tools against each other. Therefore, the purpose of this study was to determine the relationship between FMS scores and LESS scores. Ninety-eight male college athletes actively competing in sport (Gaelic games, soccer, athletics, boxing/mixed martial arts, Olympic weightlifting) participated in the study and performed the FMS and LESS screens. Both the 21-point and 100-point scoring systems were used to score the FMS. Spearman's correlation coefficients were used to determine the relationship between the 2 screening scores. The results showed a significant moderate correlation between FMS and LESS scores (rho 100 and 21 point = -0.528; -0.487; p < 0.001). In addition, r values of 0.26 and 0.23 indicate a poor shared variance between the 2 screens. The results indicate that performing well in one of the screens does not necessarily equate to performing well in the other. This has practical implications as it highlights that both screens may assess different movement patterns and should not be used as a substitute for each other.

  10. Low cost whole-organism screening of compounds for anthelmintic activity.

    Science.gov (United States)

    Preston, Sarah; Jabbar, Abdul; Nowell, Cameron; Joachim, Anja; Ruttkowski, Bärbel; Baell, Jonathan; Cardno, Tony; Korhonen, Pasi K; Piedrafita, David; Ansell, Brendan R E; Jex, Aaron R; Hofmann, Andreas; Gasser, Robin B

    2015-04-01

    Due to major problems with drug resistance in parasitic nematodes of animals, there is a substantial need and excellent opportunities to develop new anthelmintics via genomic-guided and/or repurposing approaches. In the present study, we established a practical and cost-effective whole-organism assay for the in vitro-screening of compounds for activity against parasitic stages of the nematode Haemonchus contortus (barber's pole worm). The assay is based on the use of exsheathed L3 (xL3) and L4 stages of H. contortus of small ruminants (sheep and goats). Using this assay, we screened a panel of 522 well-curated kinase inhibitors (GlaxoSmithKline, USA; code: PKIS2) for activity against H. contortus by measuring the inhibition of larval motility using an automated image analysis system. We identified two chemicals within the compound classes biphenyl amides and pyrazolo[1,5-α]pyridines, which reproducibly inhibit both xL3 and L4 motility and development, with IC50s of 14-47 μM. Given that these inhibitors were designed as anti-inflammatory drugs for use in humans and fit the Lipinski rule-of-five (including bioavailability), they show promise for hit-to-lead optimisation and repurposing for use against parasitic nematodes. The screening assay established here has significant advantages over conventional methods, particularly in terms of ease of use, throughput, time and cost. Although not yet fully automated, the current assay is readily suited to the screening of hundreds to thousands of compounds for subsequent hit-to-lead optimisation. The current assay is highly adaptable to many parasites of socioeconomic importance, including those causing neglected tropical diseases. This aspect is of major relevance, given the urgent need to deliver the goals of the London Declaration (http://unitingtocombatntds.org/resource/london-declaration) through the rapid and efficient repurposing of compounds in public-private partnerships. Copyright © 2015 Australian Society for

  11. Activity in vivo of anti-Trypanosoma cruzi compounds selected from a high throughput screening.

    Science.gov (United States)

    Andriani, Grasiella; Chessler, Anne-Danielle C; Courtemanche, Gilles; Burleigh, Barbara A; Rodriguez, Ana

    2011-08-01

    Novel technologies that include recombinant pathogens and rapid detection methods are contributing to the development of drugs for neglected diseases. Recently, the results from the first high throughput screening (HTS) to test compounds for activity against Trypanosoma cruzi trypomastigote infection of host cells were reported. We have selected 23 compounds from the hits of this HTS, which were reported to have high anti-trypanosomal activity and low toxicity to host cells. These compounds were highly purified and their structures confirmed by HPLC/mass spectrometry. The compounds were tested in vitro, where about half of them confirmed the anti-T. cruzi activity reported in the HTS, with IC50 values lower than 5 µM. We have also adapted a rapid assay to test anti-T. cruzi compounds in vivo using mice infected with transgenic T. cruzi expressing luciferase as a model for acute infection. The compounds that were active in vitro were also tested in vivo using this assay, where we found two related compounds with a similar structure and low in vitro IC50 values (0.11 and 0.07 µM) that reduce T. cruzi infection in the mouse model more than 90% after five days of treatment. Our findings evidence the benefits of novel technologies, such as HTS, for the drug discovery pathway of neglected diseases, but also caution about the need to confirm the results in vitro. We also show how rapid methods of in vivo screening based in luciferase-expressing parasites can be very useful to prioritize compounds early in the chain of development.

  12. Activity in vivo of anti-Trypanosoma cruzi compounds selected from a high throughput screening.

    Directory of Open Access Journals (Sweden)

    Grasiella Andriani

    2011-08-01

    Full Text Available Novel technologies that include recombinant pathogens and rapid detection methods are contributing to the development of drugs for neglected diseases. Recently, the results from the first high throughput screening (HTS to test compounds for activity against Trypanosoma cruzi trypomastigote infection of host cells were reported. We have selected 23 compounds from the hits of this HTS, which were reported to have high anti-trypanosomal activity and low toxicity to host cells. These compounds were highly purified and their structures confirmed by HPLC/mass spectrometry. The compounds were tested in vitro, where about half of them confirmed the anti-T. cruzi activity reported in the HTS, with IC50 values lower than 5 µM. We have also adapted a rapid assay to test anti-T. cruzi compounds in vivo using mice infected with transgenic T. cruzi expressing luciferase as a model for acute infection. The compounds that were active in vitro were also tested in vivo using this assay, where we found two related compounds with a similar structure and low in vitro IC50 values (0.11 and 0.07 µM that reduce T. cruzi infection in the mouse model more than 90% after five days of treatment. Our findings evidence the benefits of novel technologies, such as HTS, for the drug discovery pathway of neglected diseases, but also caution about the need to confirm the results in vitro. We also show how rapid methods of in vivo screening based in luciferase-expressing parasites can be very useful to prioritize compounds early in the chain of development.

  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 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.

  14. Early Sexual Intercourse: Prospective Associations with Adolescents Physical Activity and Screen Time.

    Directory of Open Access Journals (Sweden)

    Raquel Nogueira Avelar E Silva

    Full Text Available To assess the prospective associations of physical activity behaviors and screen time with early sexual intercourse initiation (i.e., before 15 years in a large sample of adolescents.We used two waves of data from the Rotterdam Youth Monitor, a longitudinal study conducted in the Netherlands. The analysis sample consisted of 2,141 adolescents aged 12 to 14 years (mean age at baseline = 12.2 years, SD = 0.43. Physical activity (e.g., sports outside school, screen time (e.g., computer use, and early sexual intercourse initiation were assessed by means of self-report questionnaires. Logistic regression models were tested to assess the associations of physical activity behaviors and screen time (separately and simultaneously with early sexual intercourse initiation, controlling for confounders (i.e., socio-demographics and substance use. Interaction effects with gender were tested to assess whether these associations differed significantly between boys and girls.The only physical activity behavior that was a significant predictor of early sexual intercourse initiation was sports club membership. Adolescent boys and girls who were members of a sports club were more likely to have had early sex (OR = 2.17; 95% CI = 1.33, 3.56. Significant gender interaction effects indicated that boys who watched TV ≥2 hours/day (OR = 2.00; 95% CI = 1.08, 3.68 and girls who used the computer ≥2 hours/day (OR = 3.92; 95% CI = 1.76, 8.69 were also significantly more likely to have engaged in early sex.These findings have implications for professionals in general pediatric healthcare, sexual health educators, policy makers, and parents, who should be aware of these possible prospective links between sports club membership, TV watching (for boys, and computer use (for girls, and early sexual intercourse initiation. However, continued research on determinants of adolescents' early sexual initiation is needed to further contribute to the strategies for improving

  15. [Screening of anti-aging active ingredients and mechanism analysis based on molecular docking technology].

    Science.gov (United States)

    Du, Ran-Feng; Zhang, Xiao-Hua; Ye, Xiao-Tong; Yu, Wen-Kang; Wang, Yun

    2016-07-01

    Dampness evil is the source of all diseases, which is easy to cause disease and promote aging, while aging could also promote the occurence and development of diseases. In this paper, the relationship between the dampness evil and aging would be discussed, to find the anti-aging active ingredients in traditional Chinese medicine (TCM), and analyze the anti-aging mechanism of dampness eliminating drug. Molecular docking technology was used, with aging-related mammalian target of rapamycin as the docking receptors, and chemical components of Fuling, Sangzhi, Mugua, Yiyiren and Houpo as the docking molecules, to preliminarily screen the anti-aging active ingredients in dampness eliminating drug. Through the comparison with active drugs already on the market (temsirolimus and everolimus), 12 kinds of potential anti-aging active ingredients were found, but their drug gability still needs further study. The docking results showed that various components in the dampness eliminating drug can play anti-aging activities by acting on mammalian target of rapamycin. This result provides a new thought and direction for the method of delaying aging by eliminating dampness. Copyright© by the Chinese Pharmaceutical Association.

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

    Directory of Open Access Journals (Sweden)

    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.

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

    Directory of Open Access Journals (Sweden)

    Oliver N F King

    2010-11-01

    Full Text Available 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.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.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.

  18. The effectiveness and cost-effectiveness of screening for active tuberculosis among migrants in the EU/EEA

    DEFF Research Database (Denmark)

    Greenaway, Christina; Pareek, Manish; Abou Chakra, Claire-Nour

    2018-01-01

    BACKGROUND: The foreign-born population make up an increasing and large proportion of tuberculosis (TB) cases in European Union/European Economic Area (EU/EEA) low-incidence countries and challenge TB elimination efforts. Methods: We conducted a systematic review to determine effectiveness (yield...... and performance of chest radiography (CXR) to detect active TB, treatment outcomes and acceptance of screening) and a second systematic review on cost-effectiveness of screening for active TB among migrants living in the EU/EEA. Results: We identified six systematic reviews, one report and three individual...... country (19-336) and screening setting (220-1,720). The CXR yield was lower (19.6 vs 336/100,000) and the numbers needed to screen were higher (5,076 vs 298) among migrants from source countries with lower TB incidence (≤ 50 compared with ≥ 350/100,000). Cost-effectiveness was highest among migrants...

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

    Directory of Open Access Journals (Sweden)

    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

  20. Yeast Estrogen Screen Assay as a Tool for Detecting Estrogenic Activity in Water Bodies

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    Mirjana Bistan

    2012-01-01

    Full Text Available The presence of endocrine-disrupting compounds in wastewater, surface water, groundwater and even drinking water has become a major concern worldwide, since they negatively affect wildlife and humans. Therefore, these substances should be effectively removed from effluents before they are discharged into surface water to prevent pollution of groundwater, which can be a source of drinking water. Furthermore, an efficient control of endocrine-disrupting compounds in wastewater based on biological and analytical techniques is required. In this study, a yeast estrogen screen (YES bioassay has been introduced and optimized with the aim to assess potential estrogenic activity of waters. First, assay duration, concentration of added substrate to the assay medium and wavelength used to measure the absorbance of the substrate were estimated. Several compounds, such as 17-β-estradiol, 17-α-ethinylestradiol, bisphenol A, nonylphenol, genisteine, hydrocortisone, dieldrin, atrazine, methoxychlor, testosterone and progesterone were used to verify its specificity and sensitivity. The optimized YES assay was sensitive and responded specifically to the selected estrogenic and nonestrogenic compounds in aqueous samples. Potential estrogenicity of influent and effluent samples of two wastewater treatment plants was assessed after the samples had been concentrated by solid-phase extraction (SPE procedure using Oasis® HLB cartridges and methanol as eluting solvent. Up to 90 % of relative estrogenic activity was detected in concentrated samples of influents to wastewater treatment plants and estrogenic activity was still present in the concentrated effluent samples. We found that the introduced YES assay is a suitable screening tool for monitoring the potential estrogenicity of effluents that are discharged into surface water.

  1. 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

    1996-07-05

    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.

  2. Application of Optical Biosensors in Small-Molecule Screening Activities

    Directory of Open Access Journals (Sweden)

    Wolfgang Knecht

    2012-03-01

    Full Text Available The last two decades have seen remarkable progress and improvements in optical biosensor systems such that those are currently seen as an important and value-adding component of modern drug screening activities. In particular the introduction of microplate-based biosensor systems holds the promise to match the required throughput without compromising on data quality thus representing a sought-after complement to traditional fluidic systems. This article aims to highlight the application of the two most prominent optical biosensor technologies, namely surface plasmon resonance (SPR and optical waveguide grating (OWG, in small-molecule screening and will present, review and discuss the advantages and disadvantages of different assay formats on these platforms. A particular focus will be on the specific advantages of the inhibition in solution assay (ISA format in contrast to traditional direct binding assays (DBA. Furthermore we will discuss different application areas for both fluidic as well as plate-based biosensor systems by considering the individual strength of the platforms.

  3. 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.

  4. 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.

  5. Physical Activity, Screen-Time Behavior, and Obesity Among 13-Year Olds in Ireland with and without Autism Spectrum Disorder.

    Science.gov (United States)

    Healy, Sean; Haegele, Justin A; Grenier, Michelle; Garcia, Jeanette M

    2017-01-01

    The primary purposes of this study were to compare (a) physical activity participation, screen-time habits, obesity, and (b) reported reasons for lack of participation in sport, between a nationally representative sample of Irish children with and without autism spectrum disorder (ASD). Participation in moderate to vigorous activity, light activity, and sports was significantly lower among the group with ASD. On examination of screen time variables, no significant differences were seen between groups. However, time spent watching TV was higher among children with ASD. Overweight or obese status was more prevalent among the group with ASD (34.4 vs. 24.7 %). The findings are discussed in relation to international statistics on youth physical activity, screen-time, and weight status, and recommendations are provided for future research.

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

    Directory of Open Access Journals (Sweden)

    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

  7. The Effect of Personal Characteristics, Perceived Threat, Efficacy and Breast Cancer Anxiety on Breast Cancer Screening Activation

    Directory of Open Access Journals (Sweden)

    Patrick De Pelsmacker

    2017-09-01

    Full Text Available In order to activate women to participate in breast cancer screening programs, a good understanding is needed of the personal characteristics that influence how women can be activated to search for more information, consult friends and doctors, and participate in breast cancer screening programs. In the current study, we investigate the effect of six personal characteristics that have in previous research been identified as important triggers of health behavior on breast cancer screening activation: Health awareness, Need for Cognition, Affect Intensity, Breast cancer knowledge, Topic involvement, and the Perceived breast cancer risk. We test the effect of these factors on four activation variables: intention of future information seeking, forwarding the message to a friend, talking to a doctor, and actual breast cancer screening attendance. Additionally, we try to unravel the process by means of which the antecedents (the six personal characteristics lead to activation. To that end, we test the mediating role of perceived breast cancer threat, perceived efficacy of screening, and the evoked breast cancer anxiety as mediators in this process. The data were collected by means of a cross-sectional survey in a sample of 700 Flemish (Belgium women who were invited to the free-of-charge breast cancer population screening. Screening attendance of this sample was provided by the government agency in charge of the organisation of the screening. Health awareness, affects intensity, topic involvement, and perceived risk have the strongest influence on activation. Breast cancer anxiety and perceived breast cancer threat have a substantial mediation effect on these effects. Efficacy perceptions are less important in the activation process. Increased health awareness and a higher level of perceived risk lead to less participation in the free of charge population based breast screening program. Implications for theory and practice are offered. The limitation

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

    Directory of Open Access Journals (Sweden)

    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.

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

    Science.gov (United States)

    Veldhuis, Lydian; van Grieken, Amy; Renders, Carry M; Hirasing, Remy A; Raat, Hein

    2014-01-01

    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. This study uses baseline data concerning 5-year-old children (n = 3067) collected for the 'Be active, eat right' study. 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. 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.

  10. Physical activity, screen time, and school absenteeism: self-reports from NHANES 2005-2008.

    Science.gov (United States)

    Hansen, Andrew R; Pritchard, Tony; Melnic, Irina; Zhang, Jian

    2016-01-01

    The purpose of this study was to examine how lifestyle behaviors in the context of physical activity levels and screen time are associated with school absenteeism. We analyzed 2005-2008 NHANES data of proxy interviews for 1048 children aged 6-11 years and in-person self-reports of 1117 adolescents aged 12-18 years. Missing 10% of school days during the past school year was defined as severe school absenteeism (SSA). Watching TV ≥2 hours a day was significantly associated with SSA among both children (OR = 3.51 [1.03-12.0]) and adolescents (OR = 3.96 [1.84-8.52]) compared with their peers watching school not included in physical activity assessment. Absenteeism was not validated with report cards. Unable to account for the absence type or frequency of illness or injury. No psychometric properties provided for subjective measures regarding participants' attitudes and characteristic traits towards physical activity, TV viewing, and school attendance. Excessive TV watching among children and adolescents, and inactivity and high activity levels (≥7 times per week) among children are independently associated with severe school absenteeism.

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

    Science.gov (United States)

    Parkash, O; Kumar, D; Kumar, S

    2015-01-01

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

  12. In vitro antioxidant activity and phytochemical screening of Garhwal Himalaya medicinal plants

    Directory of Open Access Journals (Sweden)

    Subhash Chandra

    2016-08-01

    Full Text Available Bistorta macrophylla, B.vaccinifolia and Persicaria polystachya are used for the treatment and prevention of many ailments including tuberculosis, inflammation, pyretic, fever, flue, lungs disorders, diarrhea, vomiting, arthritis, gout, kidney stones or hyperacidity and hypertension. This study was aimed to evaluate the possible in vitro antioxidant activity and phytochemical screening of B. macrophylla, B.vaccinifolia and P. polystachya. The results of antioxidant activity study of B. macrophylla showed maximum activity in the methanolic extracts at different concentration of 20, 40, 60, 80 and 100 µg/ml. The percent inhibition of writhing response by the extract was 36.18%, 44.72%, 59.21%. 67.08% and 83.39% respectively. In the present work a potent anti-oxidant activity of methanolic extract of the whole plants of B. macrophylla were demonstrated, validating the ethno pharmacological claims. These experimental findings would further establish the scientific basis of the traditional uses of the plant in the management of different conditions as well as control of different disease.

  13. Functional marine metagenomic screening for anti-quorum sensing and anti-biofilm activity.

    Science.gov (United States)

    Yaniv, Karin; Golberg, Karina; Kramarsky-Winter, Esti; Marks, Robert; Pushkarev, Alina; Béjà, Oded; Kushmaro, Ariel

    2017-01-01

    Quorum sensing (QS), a cell-to-cell communication process, entails the production of signaling molecules that enable synchronized gene expression in microbial communities to regulate myriad microbial functions, including biofilm formation. QS disruption may constitute an innovative approach to the design of novel antifouling and anti-biofilm agents. To identify novel quorum sensing inhibitors (QSI), 2,500 environmental bacterial artificial chromosomes (BAC) from uncultured marine planktonic bacteria were screened for QSI activity using soft agar overlaid with wild type Chromobacterium violaceum as an indicator. Of the BAC library clones, 7% showed high QSI activity (>40%) against the indicator bacterium, suggesting that QSI is common in the marine environment. The most active compound, eluted from BAC clone 14-A5, disrupted QS signaling pathways and reduced biofilm formation in both Pseudomonas aeruginosa and Acinetobacter baumannii. The mass spectra of the active BAC clone (14-A5) that had been visualized by thin layer chromatography was dominated by a m/z peak of 362.1.

  14. QSAR classification models for the screening of the endocrine-disrupting activity of perfluorinated compounds.

    Science.gov (United States)

    Kovarich, S; Papa, E; Li, J; Gramatica, P

    2012-01-01

    Perfluorinated compounds (PFCs) are a class of emerging pollutants still widely used in different materials as non-adhesives, waterproof fabrics, fire-fighting foams, etc. Their toxic effects include potential for endocrine-disrupting activity, but the amount of experimental data available for these pollutants is limited. The use of predictive strategies such as quantitative structure-activity relationships (QSARs) is recommended under the REACH regulation, to fill data gaps and to screen and prioritize chemicals for further experimentation, with a consequent reduction of costs and number of tested animals. In this study, local classification models for PFCs were developed to predict their T4-TTR (thyroxin-transthyretin) competing potency. The best models were selected by maximizing the sensitivity and external predictive ability. These models, characterized by robustness, good predictive power and a defined applicability domain, were applied to predict the activity of 33 other PFCs of environmental concern. Finally, classification models recently published by our research group for T4-TTR binding of brominated flame retardants and for estrogenic and anti-androgenic activity were applied to the studied perfluorinated chemicals to compare results and to further evaluate the potential for these PFCs to cause endocrine disruption.

  15. 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.

  16. Screening of antidepressant activity and estimation of quercetin from Coccinia indica using TLC densitometry.

    Science.gov (United States)

    Randhawa, Kudrat; Kumar, Deepak; Jamwal, Anupam; Kumar, Suresh

    2015-01-01

    Coccinia indica Naud (Cucurbitaceae) has been traditionally used for the treatment of depression but these claims have not been validated. The objective of this study is to investigate antidepressant activity of various extracts and fractions of C. indica aerial parts, and to estimate content of quercetin in the plant using TLC densitometry. Coccinia indica aerial parts were successively extracted using solvents in increasing order of polarity, namely n-hexane, chloroform, methanol, and water. Various extracts were evaluated for antidepressant activity at doses of 200 or 400 mg/kg, p.o., upon acute administration in mice using the forced swim test (FST). The bioactive extract was partitioned successively using solvents in increasing order of polarity, namely n-hexane, ethyl acetate, and n-butanol. All fractions were also screened for antidepressant activity at doses of 25 or 50 mg/kg, p.o., upon acute administration in mice. The methanol extract significantly reduced the duration of immobility in FST at dose of 400 mg/kg without affecting locomotor activity in open field test, thus, confirmed its antidepressant activity, which was statistically equivalent to the standard drug (imipramine, 15 mg/kg, i.p.). Ethyl acetate fraction (EAF) exhibited antidepressant activity at 50 mg/kg. Comparative TLC fingerprint studies confirmed the presence of quercetin in methanol extract and EAF. Quercetin was used as a chemical marker to standardize C. indica aerial parts using the validated TLC densitometric method, and the content of quercetin was found to be 0.00172% w/w. The present studies scientifically validated traditional claims of C. indica for antidepressant activity.

  17. Screening and identification of a Bacillus thuringiensis strain S1/4 with large and efficient insecticidal activities.

    OpenAIRE

    Jaoua, Samir; Sellami, Sameh; Zghal, Taheni; Cherif, Maroua; Zalila-Kolsi, Imen; Jaoua, Samir; Jamoussi, Kaïs

    2013-01-01

    The bacterium Bacillus thuringiensis was recognized for its entomopathogenic activities related to Cry and Cyt proteins forming the δ-endotoxins and some extracellular activities like the vegetative insecticidal proteins (VIP) and Cry1I. These activities may act specifically against diverse organisms and some of them typically characterize each strain. Here, we screened a set of 212 B. thuringiensis strains to search the higher insecticidal activities. These strains had bipyramidal and cubic ...

  18. Physical Activity, Screen-Time Behavior, and Obesity among 13-Year Olds in Ireland with and without Autism Spectrum Disorder

    Science.gov (United States)

    Healy, Sean; Haegele, Justin A.; Grenier, Michelle; Garcia, Jeanette M.

    2017-01-01

    The primary purposes of this study were to compare (a) physical activity participation, screen-time habits, obesity, and (b) reported reasons for lack of participation in sport, between a nationally representative sample of Irish children with and without autism spectrum disorder (ASD). Participation in moderate to vigorous activity, light…

  19. Clinical and microbiological effects of systemic antimicrobials combined to an anti-infective mechanical debridement for the management of aggressive periodontitis: a 12-month randomized controlled trial.

    Science.gov (United States)

    Silva-Senem, Mayra Xavier E; Heller, Débora; Varela, Victor Macedo; Torres, Maria Cynesia Barros; Feres-Filho, Eduardo Jorge; Colombo, Ana Paula Vieira

    2013-03-01

    To compare the 1-year clinical and microbiological outcomes of an enhanced anti-infective therapy with versus without systemic antimicrobials in patients with generalized aggressive periodontitis (GAP). In this 12-month randomized, double-blinded, placebo-controlled trial, 35 individuals assigned to a control (n = 17) or test group (n = 18) received full-mouth supra and subgingival ultrasonic debridement followed by scaling and root planing with chlorhexidine rinsing, brushing, and irrigation. Subjects received either amoxicillin (AMX, 500 mg) + metronidazole (MET, 250 mg) or placebos, TID for 10 days. Subgingival samples were obtained and analysed for their composition by checkerboard. Data were subjected to non-parametric tests. Both therapeutic protocols resulted in similar significant clinical improvement for most parameters at 1 year (p periodontal pathogens decreased, whereas beneficial bacteria increased in counts in both groups over time (p periodontal and other microbial pathogens were associated with disease persistence regardless treatment. The enhanced anti-infective mechanical therapy is comparable with its combination with systemic AMX+MET for most clinical parameters and for maintaining low levels of periodontal pathogens for up to 1 year after treatment of GAP. © 2012 John Wiley & Sons A/S.

  20. Isolation and screened neuroprotective active constituents from the roots and rhizomes of Valeriana amurensis.

    Science.gov (United States)

    Wang, Changfu; Xiao, Yang; Yang, Bingyou; Wang, Zhibin; Wu, Lihua; Su, Xiaolin; Brantner, Adelheid; Kuang, Haixue; Wang, Qiuhong

    2014-07-01

    In previous study, we have screened the effective fraction against Alzheimer's disease (AD-EF) from the extracts of roots and rhizomes of Valeriana amurensis, based on which neuroprotective active constituents from AD-EF were investigated. Six new compounds 1-6, including four iridoids (xiecaoside A-C and xiecaoline A), one pinane-type monoterpeneglucoside (xiecaoside D), and one phenylpropanoid glycoside (xiecaoside E) were isolated together with 11 known compounds 7-17. The structures of 1-6 were elucidated by their spectroscopic data. The protective effects of compounds 1-17 on PC12 cells with neurotoxicity induced by amyloid-beta 1-42 (Aβ(1-42)) was also investigated, respectively. Consequently, compound 6 and lignans 11-17 were responsible for protecting against Aβ-induced toxicity in PC12 cells. Copyright © 2014 Elsevier B.V. All rights reserved.

  1. Social Vulnerability as a Predictor of Physical Activity and Screen Time in European Children

    DEFF Research Database (Denmark)

    Iguacel, Isabel; Fernández-Alvira, Juan M.; Bammann, Karin

    2018-01-01

    Objectives: To examine associations between social vulnerabilities and meeting physical activity (PA) and screen time (ST) recommendations during a 2-year follow-up. Methods: 13,891 children aged 2.0 to ..., respectively. Vulnerable groups were defined at baseline as children whose parents had minimal social networks, from non-traditional families, with migrant origin or with unemployed parents. Logistic mixed-effects analyses were performed adjusting for classical socioeconomic indicators. Results: Children whose...... parents had minimal social networks had a higher risk of non-compliance with PA recommendations (subjectively assessed) at baseline. Migrants and children with unemployed parents had longer ST. All vulnerable groups were less likely to be sports club members. Conclusions: Migrants and children...

  2. 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.

  3. 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.

  4. High-Throughput Spheroid Screens Using Volume, Resazurin Reduction, and Acid Phosphatase Activity.

    Science.gov (United States)

    Ivanov, Delyan P; Grabowska, Anna M; Garnett, Martin C

    2017-01-01

    Mainstream adoption of physiologically relevant three-dimensional models has been slow in the last 50 years due to long, manual protocols with poor reproducibility, high price, and closed commercial platforms. This chapter describes high-throughput, low-cost, open methods for spheroid viability assessment which use readily available reagents and open-source software to analyze spheroid volume, metabolism, and enzymatic activity. We provide two ImageJ macros for automated spheroid size determination-for both single images and images in stacks. We also share an Excel template spreadsheet allowing users to rapidly process spheroid size data, analyze plate uniformity (such as edge effects and systematic seeding errors), detect outliers, and calculate dose-response. The methods would be useful to researchers in preclinical and translational research planning to move away from simplistic monolayer studies and explore 3D spheroid screens for drug safety and efficacy without substantial investment in money or time.

  5. Screening of the Enterocin-Encoding Genes and Antimicrobial Activity in Enterococcus Species.

    Science.gov (United States)

    Ogaki, Mayara Baptistucci; Rocha, Katia Real; Terra, MÁrcia Regina; Furlaneto, MÁrcia Cristina; Maia, Luciana Furlaneto

    2016-06-28

    In the current study, a total of 135 enterococci strains from different sources were screened for the presence of the enterocin-encoding genes entA, entP, entB, entL50A, and entL50B. The enterocin genes were present at different frequencies, with entA occurring the most frequently, followed by entP and entB; entL50A and L50B were not detected. The occurrence of single enterocin genes was higher than the occurrence of multiple enterocin gene combinations. The 80 isolates that harbor at least one enterocin-encoding gene (denoted "Gene(+) strains") were screened for antimicrobial activity. A total of 82.5% of the Gene(+) strains inhibited at least one of the indicator strains, and the isolates harboring multiple enterocin-encoding genes inhibited a larger number of indicator strains than isolates harboring a single gene. The indicator strains that exhibited growth inhibition included Listeria innocua strain CLIP 12612 (ATCC BAA-680), Listeria monocytogenes strain CDC 4555, Enterococcus faecalis ATCC 29212, Staphylococcus aureus ATCC 25923, S. aureus ATCC 29213, S. aureus ATCC 6538, Salmonella enteritidis ATCC 13076, Salmonella typhimurium strain UK-1 (ATCC 68169), and Escherichia coli BAC 49LT ETEC. Inhibition due to either bacteriophage lysis or cytolysin activity was excluded. The growth inhibition of antilisterial Gene+ strains was further tested under different culture conditions. Among the culture media formulations, the MRS agar medium supplemented with 2% (w/v) yeast extract was the best solidified medium for enterocin production. Our findings extend the current knowledge of enterocin-producing enterococci, which may have potential applications as biopreservatives in the food industry due to their capability of controlling food spoilage pathogens.

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

    Directory of Open Access Journals (Sweden)

    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.

  7. DRABAL: novel method to mine large high-throughput screening assays using Bayesian active learning

    KAUST Repository

    Soufan, Othman

    2016-11-10

    Background Mining high-throughput screening (HTS) assays is key for enhancing decisions in the area of drug repositioning and drug discovery. However, many challenges are encountered in the process of developing suitable and accurate methods for extracting useful information from these assays. Virtual screening and a wide variety of databases, methods and solutions proposed to-date, did not completely overcome these challenges. This study is based on a multi-label classification (MLC) technique for modeling correlations between several HTS assays, meaning that a single prediction represents a subset of assigned correlated labels instead of one label. Thus, the devised method provides an increased probability for more accurate predictions of compounds that were not tested in particular assays. Results Here we present DRABAL, a novel MLC solution that incorporates structure learning of a Bayesian network as a step to model dependency between the HTS assays. In this study, DRABAL was used to process more than 1.4 million interactions of over 400,000 compounds and analyze the existing relationships between five large HTS assays from the PubChem BioAssay Database. Compared to different MLC methods, DRABAL significantly improves the F1Score by about 22%, on average. We further illustrated usefulness and utility of DRABAL through screening FDA approved drugs and reported ones that have a high probability to interact with several targets, thus enabling drug-multi-target repositioning. Specifically DRABAL suggests the Thiabendazole drug as a common activator of the NCP1 and Rab-9A proteins, both of which are designed to identify treatment modalities for the Niemann–Pick type C disease. Conclusion We developed a novel MLC solution based on a Bayesian active learning framework to overcome the challenge of lacking fully labeled training data and exploit actual dependencies between the HTS assays. The solution is motivated by the need to model dependencies between existing

  8. Bidirectional associations between activity-related parenting practices, and child physical activity, sedentary screen-based behavior and body mass index: a longitudinal analysis

    OpenAIRE

    Sleddens, Ester F. C.; Gubbels, Jessica S.; Kremers, Stef P. J.; van der Plas, Eline; Thijs, Carel

    2017-01-01

    Background It has been generally assumed that activity-related parenting practices influence children?s activity behavior and weight status. However, vice versa parents may also change their parenting behaviors in response to their perceptions of their child?s activity behavior and weight status. This study examined the bidirectional relationships between activity-related parenting practices, and physical activity, sedentary screen-based behavior, and body mass index (BMI) between children?s ...

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

    International Nuclear Information System (INIS)

    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.

    2015-01-01

    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 (GI 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 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

  10. 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.

  11. 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.

  12. 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.

  13. New Human Monoamine Oxidase A Inhibitors with Potential Anti- Depressant Activity: Design, Synthesis, Biological Screening and Evaluation of Pharmacological Activity.

    Science.gov (United States)

    Evranos-Aksoz, Begum; Ucar, Gulberk; Tas, Sadik Taskin; Aksoz, Erkan; Yelekci, Kemal; Erikci, Acelya; Sara, Yildirim; Iskit, Alper Bektas

    2017-01-01

    Depression is a momentous disease that can greatly reduce the quality of life and cause death. In depression, neurotransmitter levels such as serotonine, dopamine and noradrenaline are impaired. Monoamine oxidases (MAO) are responsible for oxidative catalysis of these monoamine neurotransmitters. Because of this relation, MAO-A inhibitors show antidepressant activity by regulating neurotransmitter levels. This study was carried out to investigate the design, synthesis and activity of new antidepressant compounds in pyrazoline and hydrazone structure. Chalcones and hydrazides were heated under reflux to give new pyrazoline and hydrazone derivatives. Docking simulations were performed using AutoDock4.2. hMAO activities were determined by a fluorimetric method. To determine cell viability, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay was used. Behavioral activities of the three compounds were determined by using Forced Swim Test, Step-Through Passive Avoidance Test, Elevated Plus Maze and Open Field Arena Tests. According to in vitro tests, all of the synthesized compounds were found more potent than moclobemide and six of the synthesized compounds were found more selective than moclobemide. Three of the synthesized compounds were investigated for their behavioral activities comparing with moclobemide after 7 days of i.p. treatment at 30 mg/kg. One of the three compounds elicited significant antidepressant properties. All of the synthesized compounds were found potent hMAO-A inhibitors in in vitro screening tests. Only one of the in vivo tested three compounds, (3-(2-hydroxy-5-methylphenyl)-5- p-tolyl-4,5-dihydropyrazol-1-yl)(pyridin-4-yl) methanone indicated significant antidepressant activity. This article opens a window for further development of new pyrazoline and hydrazone derivatives as antidepressant agents. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

  14. Vitual screening and binding mode elucidation of curcumin analogues on Cyclooxygenase-2 using AYO_COX2_V1.1 protocol

    Science.gov (United States)

    Mulatsari, E.; Mumpuni, E.; Herfian, A.

    2017-05-01

    Curcumin is yellow colored phenolic compounds contained in Curcuma longa. Curcumin is known to have biological activities as anti-inflammatory, antiviral, antioxidant, and anti-infective agent [1]. Synthesis of curcumin analogue compounds has been done and some of them had biological activity like curcumin. In this research, the virtual screening of curcumin analogue compounds has been conducted. The purpose of this research was to determine the activity of these compounds as selective Cyclooxygenase-2inhibitors in in-silico. Binding mode elucidation was made by active and inactive representative compounds to see the interaction of the amino acids in the binding site of the compounds. This research used AYO_COX2_V.1.1, a structure-based virtual screening protocol (SBVS) that has been validated by Mumpuni E et al, 2014 [2]. AYO_COX2_V.1.1 protocol using a variety of integrated applications such as SPORES, PLANTS, BKchem, OpenBabel and PyMOL. The results of virtual screening conducted on 49 curcumin analogue compounds obtained 8 compounds with 4 active amino acid residues (GLY340, ILE503, PHE343, and PHE367) that were considered active as COX-2 inhibitor.

  15. Spectroscopic investigations of plasma nitriding processes: A comparative study using steel and carbon as active screen materials

    Science.gov (United States)

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

    2017-04-01

    Low-pressure pulsed DC H2-N2 plasmas were investigated in the laboratory active screen plasma nitriding monitoring reactor, PLANIMOR, to compare the usage of two different active screen electrodes: (i) a steel screen with the additional usage of CH4 as carbon containing precursor in the feeding gas and (ii) a carbon screen without the usage of any additional gaseous carbon precursor. Applying the quantum cascade laser absorption spectroscopy, the evolution of the concentration of four stable molecular species, NH3, HCN, CH4, and C2H2, has been monitored. The concentrations were found to be in a range of 1012-1016 molecules cm-3. By analyzing the development of the molecular concentrations at variations of the screen plasma power, a similar behavior of the monitored reaction products has been found for both screen materials, with NH3 and HCN as the main reaction products. When using the carbon screen, the concentration of HCN and C2H2 was 30 and 70 times higher, respectively, compared to the usage of the steel screen with an admixture of 1% CH4. Considering the concentration of the three detected hydrocarbon reaction products, a combustion rate of the carbon screen of up to 69 mg h-1 has been found. The applied optical emission spectroscopy enabled the determination of the rotational temperature of the N2+ ion which has been in a range of 650-900 K increasing with the power in a similar way in the plasma of both screens. Also with power the ionic component of nitrogen molecules, represented by the N2+ (0-0) band of the first negative system, as well as the CN (0-0) band of the violet system increase strongly in relation to the intensity of the neutral nitrogen component, i.e., the N2 (0-0) band of the second positive system. In addition, steel samples have been treated with both the steel and the carbon screen resulting in a formation of a compound layer of up to 10 wt. % nitrogen and 10 wt. % carbon, respectively, depending on the screen material.

  16. Urban Adolescents’ Physical Activity Experience, Physical Activity Levels, and Use of Screen-Based Media during Leisure Time: A Structural Model

    Science.gov (United States)

    Xie, Hui; Scott, Jason L.; Caldwell, Linda L.

    2018-01-01

    There is limited understanding of the relationship between physical activity and use of screen-based media, two important behaviors associated with adolescents’ health outcomes. To understand this relationship, researchers may need to consider not only physical activity level but also physical activity experience (i.e., affective experience obtained from doing physical activity). Using a sample predominantly consisting of African and Latino American urban adolescents, this study examined the interrelationships between physical activity experience, physical activity level, and use of screen-based media during leisure time. Data collected using self-report, paper and pencil surveys was analyzed using structural equation modeling. Results showed that physical activity experience was positively associated with physical activity level and had a direct negative relationship with use of non-active video games for males and a direct negative relationship with use of computer/Internet for both genders, after controlling for physical activity level. Physical activity level did not have a direct relationship with use of non-active video games or computer/Internet. However, physical activity level had a direct negative association with use of TV/movies. This study suggests that physical activity experience may play an important role in promoting physical activity and thwarting use of screen-based media among adolescents. PMID:29410634

  17. Urban Adolescents’ Physical Activity Experience, Physical Activity Levels, and Use of Screen-Based Media during Leisure Time: A Structural Model

    Directory of Open Access Journals (Sweden)

    Hui Xie

    2018-01-01

    Full Text Available There is limited understanding of the relationship between physical activity and use of screen-based media, two important behaviors associated with adolescents’ health outcomes. To understand this relationship, researchers may need to consider not only physical activity level but also physical activity experience (i.e., affective experience obtained from doing physical activity. Using a sample predominantly consisting of African and Latino American urban adolescents, this study examined the interrelationships between physical activity experience, physical activity level, and use of screen-based media during leisure time. Data collected using self-report, paper and pencil surveys was analyzed using structural equation modeling. Results showed that physical activity experience was positively associated with physical activity level and had a direct negative relationship with use of non-active video games for males and a direct negative relationship with use of computer/Internet for both genders, after controlling for physical activity level. Physical activity level did not have a direct relationship with use of non-active video games or computer/Internet. However, physical activity level had a direct negative association with use of TV/movies. This study suggests that physical activity experience may play an important role in promoting physical activity and thwarting use of screen-based media among adolescents.

  18. Molecular Docking and Screening Studies of New Natural Sortase A Inhibitors

    Directory of Open Access Journals (Sweden)

    Georgiana Nitulescu

    2017-10-01

    Full Text Available To date, multi-drug resistant bacteria represent an increasing health threat, with a high impact on mortality, morbidity, and health costs on a global scale. The ability of bacteria to rapidly and permanently acquire new virulence factors and drug-resistance elements requires the development of new antimicrobial agents and selection of new proper targets, such as sortase A. This specific bacterial target plays an important role in the virulence of many Gram-positive pathogens, and its inhibition should produce a mild evolutionary pressure which will not favor the development of resistance. A primary screening using a fluorescence resonance energy transfer assay was used to experimentally evaluate the inhibitory activity of several compounds on sortase A. Using molecular docking and structure-activity relationship analyses, several lead inhibitors were identified, which were further tested for antimicrobial activity using the well diffusion test and minimum inhibitory concentration. The toxicity was assessed using the Daphnia magna test and used as a future screening filter. Three natural compounds were identified in this study as promising candidates for further development into therapeutically useful anti-infective agents that could be used to treat infections caused by multi-drug resistant bacterial pathogens which include sortase A in their enzymatic set.

  19. 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.

  20. Activation of dorsolateral prefrontal cortex in a dual neuropsychological screening test: An fMRI approach

    Directory of Open Access Journals (Sweden)

    Tachibana Atsumichi

    2012-05-01

    Full Text Available Abstract Background The Kana Pick-out Test (KPT, which uses Kana or Japanese symbols that represent syllables, requires parallel processing of discrete (pick-out and continuous (reading dual tasks. As a dual task, the KPT is thought to test working memory and executive function, particularly in the prefrontal cortex (PFC, and is widely used in Japan as a clinical screen for dementia. Nevertheless, there has been little neurological investigation into PFC activity during this test. Methods We used functional magnetic resonance imaging (fMRI to evaluate changes in the blood oxygenation level-dependent (BOLD signal in young healthy adults during performance of a computerized KPT dual task (comprised of reading comprehension and picking out vowels and compared it to its single task components (reading or vowel pick-out alone. Results Behavioral performance of the KPT degraded compared to its single task components. Performance of the KPT markedly increased BOLD signal intensity in the PFC, and also activated sensorimotor, parietal association, and visual cortex areas. In conjunction analyses, bilateral BOLD signal in the dorsolateral PFC (Brodmann's areas 45, 46 was present only in the KPT. Conclusions Our results support the central bottleneck theory and suggest that the dorsolateral PFC is an important mediator of neural activity for both short-term storage and executive processes. Quantitative evaluation of the KPT with fMRI in healthy adults is the first step towards understanding the effects of aging or cognitive impairment on KPT performance.

  1. [Screening of the anti-tumor active fraction from Ipomoea batatas Lam. (cv.simon) leaves].

    Science.gov (United States)

    Lü, Shuhe; Lin, Cong; Xu, Pingsheng

    2015-05-01

    Three fractions (SM, SM-A, SM-B) were prepared from different polarity parts of Ipomoea batatas Lam. (cv.simon) leaves and the anti-tumor potency as well as the dose-response relations were evaluated. The anti-tumor activities of fraction SM, SM-A or SM-B were screened by MTS in human hepatic cancer Hep3B cells, lung cancer A549 cells or gastric carcinoma MGC803 cells, respectively. The three fractions all showed anti-tumor activities in three cancer cells with different sensitivity. Among them, SM-B was the most potent fraction with IC50 values at 15.17 mg/L, 72.64 mg/L or 165.47 mg/L in MGC803 cells, A549 cells or Hep3B cells, respectively (P<0.05). Th e extraction of Brazil sweet potato leaves displayed anti-tumor activity and SM-B was the most potent fraction.

  2. Computational screening for active compounds targeting protein sequences: methodology and experimental validation.

    Science.gov (United States)

    Wang, Fei; Liu, Dongxiang; Wang, Heyao; Luo, Cheng; Zheng, Mingyue; Liu, Hong; Zhu, Weiliang; Luo, Xiaomin; Zhang, Jian; Jiang, Hualiang

    2011-11-28

    The three-dimensional (3D) structures of most protein targets have not been determined so far, with many of them not even having a known ligand, a truly general method to predict ligand-protein interactions in the absence of three-dimensional information would be of great potential value in drug discovery. Using the support vector machine (SVM) approach, we constructed a model for predicting ligand-protein interaction based only on the primary sequence of proteins and the structural features of small molecules. The model, trained by using 15,000 ligand-protein interactions between 626 proteins and over 10,000 active compounds, was successfully used in discovering nine novel active compounds for four pharmacologically important targets (i.e., GPR40, SIRT1, p38, and GSK-3β). To our knowledge, this is the first example of a successful sequence-based virtual screening campaign, demonstrating that our approach has the potential to discover, with a single model, active ligands for any protein.

  3. Diversity and screening for antimicrobial activity of endophytic fungi from Alstonia scholaris.

    Science.gov (United States)

    Mahapatra, S; Banerjee, D

    2010-09-01

    Endophytic fungi of three tissues (petiole, bark and leaf) of Alstonia scholaris were assessed. A total number of 1,152 endophytic fungi were isolated from 1,002 different plant segments of seven different localities of Paschim Medinipur, West Bengal, India. The isolated fungi belong to nineteen genera, including four unidentified fungi and yeast. Colletotrichum sp. (20.39%) and Sordaria sp. (29.68%) were most commonly isolated from this plant. Hyalopus sp., Fusarium sp. and Curvularia sp. were also isolated. The colonization frequency of endophytic fungi is much higher in leaves (44.66%) in comparison to petioles (32.16%) and barks (23.17%). The study provided evidence for tissue specificity of endophytic fungi. The endophytic fungal species diversity was higher in plant segments collected from Gopegarh and Khoirullahchak, while diversity was the lowest in Rice mill area. Screenings of antimicrobial activity of these isolated endophytic fungi were done. Eight endophytic fungi showed antimicrobial activity. Among them Curvularia sp., Aspergillus sp. and one unidentified fungus showed maximum activity against test pathogens.

  4. In vitro bioassays to screen for endocrine active pharmaceuticals in surface and waste waters.

    Science.gov (United States)

    Kunz, Petra Y; Kienle, Cornelia; Carere, Mario; Homazava, Nadzeya; Kase, Robert

    2015-03-15

    In the context of the European Water Framework Directive (WFD) it is fully recognized that pharmaceuticals can represent a relevant issue for the achievement of the good chemical and ecological status of European surface water bodies. The recent European Directive on the review of priority substances in surface water bodies has included three pharmaceuticals of widespread use (diclofenac, 17α-ethinylestradiol (EE2), 17β-estradiol (E2)) in the European monitoring list, the so-called watch list. Endocrine active pharmaceuticals such as EE2 and E2 (also occurring as natural hormone) can cause adverse effects on aquatic ecosystems at very low levels. However, monitoring of these pharmaceuticals within the watch list mechanism of the WFD and national monitoring programs can be difficult because of detection problems of most routine analytical methods. With proposed annual average Environmental Quality Standards (AA-EQS) of 0.035 ng/L and 0.4 ng/L, respectively, the estrogenic pharmaceutical EE2 and the natural hormone E2 are among those substances. Sensitive in vitro bioassays could reduce the current detection problems by measuring the estrogenic activity of environmental samples. In a short review article the application of this approach to screen and assess the risks of endocrine active pharmaceuticals with a focus on estrogenic pharmaceuticals in environmental waters is discussed. Copyright © 2014 Elsevier B.V. All rights reserved.

  5. 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. Copyright © 2012 John Wiley & Sons, Ltd.

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

    Directory of Open Access Journals (Sweden)

    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.

  7. Screening for Neuraminidase Inhibitory Activity in Traditional Chinese Medicines Used to Treat Influenza.

    Science.gov (United States)

    Yang, Xian-Ying; Liu, Ai-Lin; Liu, Shu-Jing; Xu, Xiao-Wei; Huang, Lin-Fang

    2016-08-27

    To screen for influenza virus neuraminidase inhibition and to provide a reference for the clinical treatment of influenza using traditional Chinese medicines (TCM). In this study, 421 crude extracts (solubilized with petroleum ether, ethanol, ethyl acetate, and aqueous solvents) were obtained from 113 TCM. The medicine extracts were then reacted with oseltamivir, using 2'-(4-methylumbelliferyl)-α-D-N-acetylneuraminic acid (MUNANA) as the substrate, to determine influenza virus neuraminidase activity using a standard fluorimetric assay. It was found that Chinese medicine extracts from Pyrola calliantha, Cynanchum wilfordii, Balanophora involucrata and Paeonia delavayi significantly inhibited neuraminidase activity at a concentration of 40 μg/mL. Dose-dependent inhibitory assays also revealed significant inhibition. The IC50 range of the TCM extracts for influenza virus neuraminidase was approximately 12.66-34.85 μg/mL, respectively. Some Chinese medicines have clear anti-influenza viral effects that may play an important role in the treatment of influenza through the inhibition of viral neuraminidase. The results of this study demonstrated that plant medicines can serve as a useful source of neuraminidase (NA) inhibitors and further investigation into the pharmacologic activities of these extracts is warranted.

  8. Brazilian red propolis: phytochemical screening, antioxidant activity and effect against cancer cells.

    Science.gov (United States)

    de Mendonça, Izabel Cristina Gomes; Porto, Isabel Cristina Celerino de Moraes; do Nascimento, Ticiano Gomes; de Souza, Naiana Soares; Oliveira, José Marcos dos Santos; Arruda, Rodolfo Elleson dos Santos; Mousinho, Kristiana Cerqueira; dos Santos, Aldenir Feitosa; Basílio-Júnior, Irinaldo Diniz; Parolia, Abhishek; Barreto, Francisco Stefânio

    2015-10-14

    The implementation of new public healthcare models that stimulate the use of natural products from traditional medicine, as a so-called integrated medicine, refers to an approach that use best of both conventional medicine and traditional medicine. Propolis is a widely used natural product by different ancient cultures and known to exhibit biological activities beneficial for health. The large number of studies conducted with propolis had shown that its chemical composition differs as a function of the climate, plant diversity and bee species and plays an important role on its therapeutic properties. The aim of this study was to analyse the phytochemical profile of the ethanolic extract of red propolis (EEP) and its fractionation, antioxidant action of EEP and its fractions hexane, cloroform and ethyl acetate and cytotoxic activity of EEP on human tumour cell lines SF-295 (glioblastoma), OVCAR-8 (ovary) and HCT-116 (colon). EEP was obtained by maceration with absolute ethanol, then it was concentrated in rotaevaporator up to complete evaporation of the solvent. The crude extract was fractionated with hexane, ethyl acetate, chloroform and methanol and they were subjected to phytochemical screening and total phenolic compounds. Antioxidant activity of EEP and fractions was done by means of the 2,2-diphenyl-1-picryhydrazyl (DPPH) method. Biomarkers of red propolis were identified by LC-Orbitrap-FTMS. To assess cytotoxic activity of the extract, cells were exposed to EEP over 72 h. Cell viability was assessed by means of MTT assay. The percentage of cell growth inhibition (IC50) was analysed by means of non-linear regression, and the absorbance values of the various investigated concentrations were subjected to one-factor analysis of variance (ANOVA) followed by Tukey's or Tamhane's tests (α = 0.05). The results obtained using phytochemical screening and LC-Orbitrap-FTMS indicated the presence of phlobaphene tannins, catechins, chalcones, aurones, flavonones

  9. Development of HomeSTEAD's physical activity and screen time physical environment inventory.

    Science.gov (United States)

    Hales, Derek; Vaughn, Amber E; Mazzucca, Stephanie; Bryant, Maria J; Tabak, Rachel G; McWilliams, Christina; Stevens, June; Ward, Dianne S

    2013-12-05

    The home environment has a significant influence on children's physical activity, sedentary behavior, dietary intake, and risk for obesity and chronic disease. Our understanding of the most influential factors and how they interact and impact child behavior is limited by current measurement tools, specifically the lack of a comprehensive instrument. HomeSTEAD (the Home Self-administered Tool for Environmental assessment of Activity and Diet) was designed to address this gap. This new tool contains four sections: home physical activity and media equipment inventory, family physical activity and screen time practices, home food inventory, and family food practices. This paper will describe HomeSTEAD's development and present reliability and validity evidence for the first section. The ANGELO framework guided instrument development, and systematic literature reviews helped identify existing items or scales for possible inclusion. Refinement of items was based on expert review and cognitive interviews. Parents of children ages 3-12 years (n = 125) completed the HomeSTEAD survey on three separate occasions over 12-18 days (Time 1, 2, and 3). The Time 1 survey also collected demographic information and parent report of child behaviors. Between Time 1 and 2, staff conducted an in-home observation and measured parent and child BMI. Kappa and intra-class correlations were used to examine reliability (test-retest) and validity (criterion and construct). Reliability and validity was strong for most items (97% having ICC > 0.60 and 72% having r > 0.50, respectively). Items with lower reliability generally had low variation between people. Lower validity estimates (r parents. Small to moderate, but meaningful, correlations between physical environment factors and BMI, outside time, and screen time were observed (e.g., amount of child portable play equipment in good condition and easy to access was significantly associated with child BMI: r = -0.23), providing evidence of

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

    International Nuclear Information System (INIS)

    Khairusy Syakirah Zulkifli; Noriham Abdullah; Aminah Abdullah; Nurain Aziman; Wan Saidatul Syida Wan Kamarudin

    2012-01-01

    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, EC 50 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)

  11. Screening the antifungal activity of essential oils against decay fungi from palmyrah leaf handicrafts

    Directory of Open Access Journals (Sweden)

    Subajini Mahilrajan

    2014-01-01

    Full Text Available BACKGROUND: The whitish tender leaves of Palmyrah are used for making handicrafts. The problem with these articles is discolouration with time and become more brittle due to fungal attack. This could be prevented by some protective coating. Instead of expensive and harmful chemicals we decided to test natural plant essential oils to control fungal attack. Palmyrah leaf article decay fungi were isolated from two different sites of Jaffna peninsula. In this investigation Antifungal Activity of different plant essential oils from neem (Azadirachta indica, castor (Ricinus communis, citronella (Cymbopogon sp and camphor (Cinnamomum camphora obtained from local market have been evaluated against isolated fungi. For screening of Antifungal activity, tests and controls were set to determine minimum inhibitory concentration (MIC and Percentage of Growth Inhibition. RESULTS: Morphologically three different types of Palmyrah leaf decay fungi were isolated and characterized asAspergillus niger, Aspergillus flavus and Penicillium sp. Neem and castor oils have recorded no significant (0.05 > P antifungal activity while citronella and camphor oils showed significantly different antifungal activity compared with control. Camphor oil and Citronella oil showed 100, 58.13% of average growth inhibition for A. niger. 96.38, 51.32% for A.flavus and 84.99, 72.76% forPenicillium sp respectively. Camphor oil showed highest percentage of growth inhibition at lowest minimum inhibitory concentration compared with citronella oil. Camphor oil was found to be highly antifungal and most effective against A niger, and A. flavus, compared with Penicillium sp and gave 100 percentage of growth inhibitions at 5, 1 and 15 ml/dl minimum inhibitory concentration respectively. CONCLUSION: Significantly higher broad-spectrum of antifungal activity was observed in camphor oil than other tested oils because it showed highest percentage of growth inhibition at lowest inhibitory

  12. Screening for proteolytically active lactic acid bacteria and bioactivity of peptide hydrolysates obtained with selected strains.

    Science.gov (United States)

    Kliche, T; Li, B; Bockelmann, W; Habermann, D; Klempt, M; de Vrese, M; Wutkowski, A; Clawin-Raedecker, I; Heller, K J

    2017-10-01

    In a screening for proteolytically active lactic acid bacteria, three strains, Lactobacillus delbrueckii ssp. lactis 92202, Lactobacillus helveticus 92201, and Lactobacillus delbrueckii ssp. bulgaricus 92059, showed the highest activities following growth in milk. All three strains degraded α- and β-casein, but did not hydrolyse κ-casein. HPLC analysis of skim milk fermentation revealed increasing amounts of peptides after 5 and 10 h with Lb. d. ssp. bulgaricus 92059. Hydrolysates obtained with Lb. d. ssp. lactis 92202 and Lb. d. ssp. bulgaricus 92059 revealed the highest angiotensin-converting enzyme-inhibitory effect. The effect was dose dependent. Almost no effect (<10%) was seen for Lb. helveticus 92201. For Lb. d. ssp. bulgaricus 92059, maximal inhibition of approx. 65% was reached after 25 h of fermentation. In an in vitro assay measuring potential immunomodulation, hydrolysates of the three strains yielded anti-inflammatory activities in the presence of TNF-α. However, the effects were more pronounced at lower hydrolysate concentrations. In the absence of TNF-α, slight pro-inflammatory effects were observed. The hydrolysate of Lb. d. ssp. bulgaricus 92059, when purified by means of solid-phase extraction, exhibited pro-inflammatory activity. Sour whey containing Lb. d. ssp. bulgaricus 92059 cells showed pro-inflammatory activity while cell-free sour whey was clearly anti-inflammatory. In the purified hydrolysate, 20 different α- and β-casein (CN)-derived peptides could be identified by LC-MS. Most peptides originated from the central and C-terminal regions of β-casein. Peptide length was between 9 (β-CN(f 59-67)) and 22 amino acids (β-CN(f 117-138)).

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

    Directory of Open Access Journals (Sweden)

    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.

  14. 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. Copyright © 2014 The Foundation for Professionals in Services for Adolescents. Published by Elsevier Ltd. All rights reserved.

  15. 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

  16. Bidirectional associations between activity-related parenting practices, and child physical activity, sedentary screen-based behavior and body mass index: a longitudinal analysis.

    Science.gov (United States)

    Sleddens, Ester F C; Gubbels, Jessica S; Kremers, Stef P J; van der Plas, Eline; Thijs, Carel

    2017-07-06

    It has been generally assumed that activity-related parenting practices influence children's activity behavior and weight status. However, vice versa parents may also change their parenting behaviors in response to their perceptions of their child's activity behavior and weight status. This study examined the bidirectional relationships between activity-related parenting practices, and physical activity, sedentary screen-based behavior, and body mass index (BMI) between children's age of 5 and 7 years. Three scales of the Activity-related Parenting Questionnaire (i.e. 'restriction of sedentary behavior', 'stimulation of physical activity', and 'monitoring of physical activity') were completed by 1694 parents of the Dutch KOALA Birth Cohort Study at the child's age of around 5 and again around age 7. Physical activity, sedentary screen-based behavior and BMI were measured at both ages as well. Linear regression models were used to estimate the bidirectional associations between each parenting practice and the child's physical activity levels, sedentary screen-based behavior and BMI z-scores. Several parenting practices at age 5 predicted child physical activity, sedentary screen-based behavior, and BMI z-scores at age 7. Restriction of sedentary behavior positively predicted child BMI and sedentary screen-based behavior, whereas this practice negatively predicted child physical activity. In addition, stimulation of physical activity at age 5 was significantly associated with higher levels of child physical activity at age 7. The following child factors at age 5 predicted parenting practices at age 7: Child physical activity positively predicted parental stimulation of physical activity and monitoring activities. Sedentary screen-based behavior was associated with lower parental stimulation to be active. Findings generally revealed that parents and children mutually influence each other's behavior. A reinforcing feedback loop was present between parental stimulation

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

    International Nuclear Information System (INIS)

    Chen, Li; Schmidt, Emmett V; Stuart, Lynda; Ohsumi, Toshiro K; Burgess, Shawn; Varshney, Gaurav K; Dastur, Anahita; Borowsky, Mark; Benes, Cyril; Lacy-Hulbert, Adam

    2013-01-01

    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

  18. 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

  19. Correlating In Vitro Target-Oriented Screening and Docking: Inhibition of Matrix Metalloproteinases Activities by Flavonoids.

    Science.gov (United States)

    Crascì, Lucia; Basile, Livia; Panico, Annamaria; Puglia, Carmelo; Bonina, Francesco P; Basile, Pierluigi Maria; Rizza, Luisa; Guccione, Salvatore

    2017-07-01

    Metalloproteases are a family of zinc-containing endopeptidases involved in a variety of pathological disorders. The use of flavonoid derivatives as potential metalloprotease inhibitors has recently increased.Particular plants growing in Sicily are an excellent yielder of the flavonoids luteolin, apigenin, and their respective glycoside derivatives (7-O-rutinoside, 7-O-glucoside, and 7-O-glucuronide).The inhibitory activity of luteolin, apigenin, and their respective glycoside derivatives on the metalloproteases MMP-1, MMP-3, MMP-13, MMP-8, and MMP-9 was assessed and rationalized correlating in vitro target-oriented screening and in silico docking.The flavones apigenin, luteolin, and their respective glucosides have good ability to interact with metalloproteases and can also be lead compounds for further development. Glycones are more active on MMP-1, -3, -8, and -13 than MMP-9. Collagenases MMP-1, MMP-8, and MMP-13 are inhibited by compounds having rutinoside glycones. Apigenin and luteolin are inactive on MMP-1, -3, and -8, which can be interpreted as a better selectivity for both -9 and -13 peptidases. The more active compounds are apigenin-7-O-rutinoside on MMP-1 and luteolin-7-O-rutinoside on MMP-3. The lowest IC 50 values were also found for apigenin-7-O-glucuronide, apigenin-7-O-rutinoside, and luteolin-7-O-glucuronide. The glycoside moiety might allow for a better anchoring to the active site of MMP-1, -3, -8, -9, and -13. Overall, the in silico data are substantially in agreement with the in vitro ones (fluorimetric assay). Georg Thieme Verlag KG Stuttgart · New York.

  20. Screening of endophytic fungi having ability for antioxidative and alpha-glucosidase inhibitor activities isolated from Taxus sumatrana.

    Science.gov (United States)

    Artanti, N; Tachibana, S; Kardono, L B S; Sukiman, H

    2011-11-15

    Endophytic microbes are considered as an important source of natural products. They show antibiotic, anticancer, antioxidative and antidiabetic activities. Therefore, there are many reports on the isolation and bioactivity screening of endophytic fungi from various plants including Taxus species. Taxus sumatrana (Miq.) de Laub is found in Indonesia. The objective of this study is to conduct an in vitro screening of 14 endophytic fungi isolated from Taxus sumatrana having antioxidative and alpha-glucosidase inhibitor activities. Each endophytic fungus was cultured for 7 days and the fungal mycelium and medium were extracted with methanol and ethyl acetate, respectively, to produce each extract. The antioxidative activity of each extract was tested by DPPH free radical scavenging activity and beta-carotene bleaching assays, whereas antidiabetic activity was tested based on alpha-glucosidase inhibitor activity. The screening results showed that fungal mycelia of TSC 13 had the best alpha-glucosidase inhibitor activity and TSC 24 had the best antioxidative activity. Isolation of bioactive compounds from TSC 13 and TSC 24 is being conducted. This is the first report that endophytic fungi isolated from T. sumatrana exhibited anti alpha-glucosidase inhibitory and anti oxidative activities.

  1. Physical activity, screen time and self-rated health and mental health in Canadian adolescents.

    Science.gov (United States)

    Herman, Katya M; Hopman, Wilma M; Sabiston, Catherine M

    2015-04-01

    Physical activity (PA) and screen time (ST) are associated with self-rated health (SRH) in adults; however, SRH has been less studied among youth, and information about self-rated mental health (SRMH) is lacking. This study examined the associations of PA and ST with SRH and SRMH among adolescents. Cross-sectional data from the 2011-2012 Canadian Community Health Survey included 7725 participants aged 12-17years, representing 1,820,560 Canadian adolescents. Associations of self-reported PA and ST to SRH and SRMH were assessed, controlling for age, race/ethnicity, smoking, highest household education and weight status. Excellent/very good SRH was reported by 78% of active vs. 62% of inactive adolescents, and 77% of those meeting vs. 70% of those exceeding ST guidelines (both pactive vs. 76% of inactive adolescents, and 84% of those meeting vs. 78% of those exceeding ST guidelines (both phealth perceptions among Canadian adolescents. Interventions should consider health perceptions in addition to biomedical outcomes. Copyright © 2015 Elsevier Inc. All rights reserved.

  2. Screening of plant resources with anti-ice nucleation activity for frost damage prevention.

    Science.gov (United States)

    Suzuki, Shingo; Fukuda, Satoshi; Fukushi, Yukiharu; Arakawa, Keita

    2017-11-01

    Previous studies have shown that some polyphenols have anti-ice nucleation activity (anti-INA) against ice-nucleating bacteria that contribute to frost damage. In the present study, leaf disk freezing assay, a test of in vitro application to plant leaves, was performed for the screening of anti-INA, which inhibits the ice nucleation activity of an ice-nucleating bacterium Erwinia ananas in water droplets on the leaf surfaces. The application of polyphenols with anti-INA, kaempferol 7-O-β-glucoside and (-)-epigallocatechin gallate, to the leaf disk freezing assay by cooling at -4--6 °C for 3 h, revealed that both the compounds showed anti-INAs against E. ananas in water droplets on the leaf surfaces. Further, this assay also revealed that the extracts of five plant leaves showed high anti-INA against E. ananas in water droplets on leaf surfaces, indicating that they are the candidate resources to protect crops from frost damage.

  3. Amazonian plant crude extract screening for activity against multidrug-resistant bacteria.

    Science.gov (United States)

    Correia, A F; Segovia, J F O; Gonçalves, M C A; de Oliveira, V L; Silveira, D; Carvalho, J C T; Kanzaki, L I B

    2008-01-01

    Antimicrobial resistance is a subject of great concern in public health and also in the designing of strategies for current therapeutic protocols all over the world. New drugs, including those necessary for a reserve armamentarium and exhibiting less side effects deserve special attention. In rural areas, particularly in Brazil, a huge number of natural products, in different artisanal preparations, mainly from plants, have been used by traditional populations to cure diseases. Despite some of these plants have been studied, many of them are awaiting to have their compounds chemically characterized and investigated their pharmacodynamics properties. Further, as well known, the environment plays a crucial role in the metabolism of these plants, yielding different and varied molecular complexes depending on the period of collection, climate conditions, kind of soil and also the plant speciation. In this report, ethanol crude extract of 10 different botanical specimens from the Amazon region of Brazil, in the Amapa State, were screened for antibacterial activity of 7 clinical resistant microorganisms utilizing as control ATCC bacterial species by the Kirby-Bauer method. Plant extracts of Geissospermum argenteum, Uncaria guianensis, Brosimum acutifolium, Copaifera reticulate, Licania macrophylla, Ptycopetalum olacoides and Dalbergia subcymosa yielded activity against Staphylococcus aureus and Pseudomonas aeruginosa, both multidrug resistant, and Staphylococcus aureus ATCC strain.

  4. In silico Screening and Evaluation of the Anticonvulsant Activity of Docosahexaenoic Acid-Like Molecules in Experimental Models of Seizures.

    Science.gov (United States)

    Gharibi Loron, Ali; Sardari, Soroush; Narenjkar, Jamshid; Sayyah, Mohammad

    2017-01-01

    Resistance to antiepileptic drugs and the intolerability in 20-30% of the patients raises demand for developing new drugs with improved efficacy and safety. Acceptable anticonvulsant activity, good tolerability, and inexpensiveness of docosahexaenoic acid (DHA) make it as a good candidate for designing and development of the new anticonvulsant medications. Ten DHA-based molecules were screened based on in silico screening of DHA-like molecules by root-mean-square deviation of atomic positions, the biological activity score of Professional Association for SQL Server, and structural requirements suggested by pharmacophore design. Anticonvulsant activity was tested against clonic seizures induced by pentylenetetrazole (PTZ, 60 mg/kg, i.p.) and tonic seizures induced by maximal electroshock (MES, 50 mA, 50 Hz, 1 ms duration) by intracerebroventricular (i.c.v.) injection of the screened compounds to mice. Among screened compounds, 4-Phenylbutyric acid, 4-Biphenylacetic acid, phenylacetic acid, and 2-Phenylbutyric acid showed significant protective activity in pentylenetetrazole test with ED50 values of 4, 5, 78, and 70 mM, respectively. In MES test, shikimic acid and 4-tert-Butylcyclo-hexanecarboxylic acid showed significant activity with ED50 values 29 and 637 mM, respectively. Effective compounds had no mortality in mice up to the maximum i.c.v. injectable dose of 1 mM. Common electrochemical features and three-dimensional spatial structures of the effective compounds suggest the involvement of the anticonvulsant mechanisms similar to the parent compound DHA.

  5. The association between recreational physical activity, sedentary time, and colorectal polyps in a population screened for colorectal cancer.

    Science.gov (United States)

    Brenner, Darren R; Shaw, Eileen; Yannitsos, Demetra H; Warkentin, Matthew T; Brockton, Nigel T; McGregor, S Elizabeth; Town, Susanna; Hilsden, Robert J

    2018-04-01

    Regular recreational moderate to vigorous physical activity (rMVPA) has been previously associated with a reduced risk of colorectal cancer (CRC), however, few studies have examined the association of rMVPA with colorectal polyps, the pre-malignant precursor lesions. The objective of this study was to examine the associations between physical activity and sitting time and polyps at the time of screening. We conducted a cross-sectional study of 2496 individuals undergoing screening-related colonoscopy in Calgary, Alberta, Canada. Physical activity and sitting time were characterized using hours of rMVPA, meeting physical activity recommendations and hours of sitting time using self-reported data obtained from the International Physical Activity Questionnaire. Logistic regression models were used to estimate the crude and adjusted odds ratios (OR) for presence of polyps associated with rMVPA and sitting time. Meeting physical activity guidelines of ≥150 min/week was non-significantly associated with a modest decrease in odds of having ≥1 polyp at screening (OR adj  = 0.95, 95% CI: 0.80-1.14). In males, threshold effects for sitting time were observed for up to 20 h/week (OR adj per hour sitting = 1.07, 95% CI: 1.01-1.13). In stratified analysis, larger inverse associations were observed between physical activity and the presence of polyps in females, obese individuals, and ever smokers, compared to pooled findings. In this large CRC screening population, there was a suggestive association between increased rMVPA and reduced prevalence of polyps at screening, particularly among females. Even low amounts of regular sitting time (0-20 h/day) were associated with the presence of polyps, particularly among males. Further research on rMVPA and sitting time is necessary to better inform strategies to reduce the frequency of pre-malignant colorectal lesions. Copyright © 2018 Elsevier Ltd. All rights reserved.

  6. Does home equipment contribute to socioeconomic gradients in Australian children's physical activity, sedentary time and screen time?

    Science.gov (United States)

    Dumuid, Dot; Olds, Timothy S; Lewis, Lucy K; Maher, Carol

    2016-08-05

    Activity behaviours (physical activity, sedentary time and screen time) have been linked to health outcomes in childhood. Furthermore, socioeconomic disparities have been observed in both children's activity behaviours and health outcomes. Children's physical home environments may play a role in these relationships. This study aimed to examine the associations and interactions between children's physical home environment, socioeconomic status and moderate-to-vigorous physical activity, sedentary time and screen time. Australian children (n = 528) aged 9-11 years from randomly selected schools participated in the cross-sectional International Study of Childhood Obesity, Lifestyle and the Environment. Children's physical home environment (access to equipment), socioeconomic status (household income and parental education) and demographic variables (gender and family structure) were determined by parental questionnaire. Moderate-to-vigorous physical activity and sedentary time were measured objectively by 7-day 24-h accelerometry. Screen time was obtained from child survey. The associations between the physical home environment, socioeconomic status and moderate-to-vigorous physical activity, sedentary time and screen time were examined for 427 children, using analysis of covariance, and linear and logistic regression, with adjustment for gender and family structure. The presence of TVs (p music devices (p = 0.04) was significantly and positively associated with screen time. Ownership of these devices (with the exception of music devices) was inversely related to socioeconomic status (parental education). Children's moderate-to-vigorous intensity physical activity (p = 0.04) and possession of active play equipment (p = 0.04) were both positively associated with socioeconomic status (household income), but were not related to each other (with the exception of bicycle ownership). Children with less electronic devices, particularly in their bedrooms

  7. Does home equipment contribute to socioeconomic gradients in Australian children’s physical activity, sedentary time and screen time?

    Directory of Open Access Journals (Sweden)

    Dot Dumuid

    2016-08-01

    Full Text Available Abstract Background Activity behaviours (physical activity, sedentary time and screen time have been linked to health outcomes in childhood. Furthermore, socioeconomic disparities have been observed in both children’s activity behaviours and health outcomes. Children’s physical home environments may play a role in these relationships. This study aimed to examine the associations and interactions between children’s physical home environment, socioeconomic status and moderate-to-vigorous physical activity, sedentary time and screen time. Methods Australian children (n = 528 aged 9–11 years from randomly selected schools participated in the cross-sectional International Study of Childhood Obesity, Lifestyle and the Environment. Children’s physical home environment (access to equipment, socioeconomic status (household income and parental education and demographic variables (gender and family structure were determined by parental questionnaire. Moderate-to-vigorous physical activity and sedentary time were measured objectively by 7-day 24-h accelerometry. Screen time was obtained from child survey. The associations between the physical home environment, socioeconomic status and moderate-to-vigorous physical activity, sedentary time and screen time were examined for 427 children, using analysis of covariance, and linear and logistic regression, with adjustment for gender and family structure. Results The presence of TVs (p < 0.01 and video game consoles (p < 0.01 in children’s bedrooms, and child possession of handheld video games (p = 0.04, cell phones (p < 0.01 and music devices (p = 0.04 was significantly and positively associated with screen time. Ownership of these devices (with the exception of music devices was inversely related to socioeconomic status (parental education. Children’s moderate-to-vigorous intensity physical activity (p = 0.04 and possession of active play equipment (p = 0.04 were

  8. In vivo analgesic activity, toxicity and phytochemical screening of the hydroalcoholic extract from the leaves of Psidium cattleianum Sabine.

    Science.gov (United States)

    Alvarenga, Felipe Queiroz; Mota, Bárbara C F; Leite, Marcel N; Fonseca, Jaciara M S; Oliveira, Dario A; Royo, Vanessa de Andrade; e Silva, Márcio L A; Esperandim, Viviane; Borges, Alexandre; Laurentiz, Rosangela S

    2013-10-28

    Psidium cattleianum Sabine is extensively used in Brazilian traditional medicine to treat several diseases including painful disorders. Aim of the study to investigate the toxicity and the possible analgesic activities of the hydroalcoholic extract from the leaves of Psidium cattleianum Sabine (ELPCS), to support its use in folk medicine. To screen the major phytochemical constituents of this extract and evaluate their antioxidant activity. ELPCS was assessed for its antioxidant activity using the DPPH model. Its analgesic activity was examined using mouse models of acetic acid-induced writhing and hot plate paw licking models. The major phytochemical constituents of the extract were screened; their toxicity on LLC-MK2 mammalian cells was evaluated. ELPCS exhibited significant peripheral analgesic activity at doses of 60, 80, 100, 200 and 400mg/kg in mice, but it did not display central analgesic activity and not was toxic to LLC-MK2 cell (LD50>400 µg/mL). The extract exhibited free radical scavenging activity as evidenced by IC50 values (15.9 µg/mL) obtained by the DPPH method. Phytochemical screening detected flavonoids, saponins, cardiac glycosides, anthraquinones, and tannins. The results of the experimental studies proved the analgesic activity of ELPCS and supported the traditional use of this plant. © 2013 Elsevier Ireland Ltd. All rights reserved.

  9. The Functional Movement Screen and Injury Risk: Association and Predictive Value in Active Men.

    Science.gov (United States)

    Bushman, Timothy T; Grier, Tyson L; Canham-Chervak, Michelle; Anderson, Morgan K; North, William J; Jones, Bruce H

    2016-02-01

    The Functional Movement Screen (FMS) is a series of 7 tests used to assess the injury risk in active populations. To determine the association of the FMS with the injury risk, assess predictive values, and identify optimal cut points using 3 injury types. Cohort study; Level of evidence, 2. Physically active male soldiers aged 18 to 57 years (N = 2476) completed the FMS. Demographic and fitness data were collected by survey. Medical record data for overuse injuries, traumatic injuries, and any injury 6 months after the FMS assessment were obtained. Sensitivity, specificity, positive predictive value (PPV), and negative predictive value (NPV) were calculated along with the receiver operating characteristic (ROC) to determine the area under the curve (AUC) and identify optimal cut points for the risk assessment. Risks, risk ratios (RRs), odds ratios (ORs), and 95% CIs were calculated to assess injury risks. Soldiers who scored ≤14 were at a greater risk for injuries compared with those who scored >14 using the composite score for overuse injuries (RR, 1.84; 95% CI, 1.63-2.09), traumatic injuries (RR, 1.26; 95% CI, 1.03-1.54), and any injury (RR, 1.60; 95% CI, 1.45-1.77). When controlling for other known injury risk factors, multivariate logistic regression analysis identified poor FMS performance (OR [score ≤14/19-21], 2.00; 95% CI, 1.42-2.81) as an independent risk factor for injuries. A cut point of ≤14 registered low measures of predictive value for all 3 injury types (sensitivity, 28%-37%; PPV, 19%-52%; AUC, 54%-61%). Shifting the injury risk cut point of ≤14 to the optimal cut points indicated by the ROC did not appreciably improve sensitivity or the PPV. Although poor FMS performance was associated with a higher risk of injuries, it displayed low sensitivity, PPV, and AUC. On the basis of these findings, the use of the FMS to screen for the injury risk is not recommended in this population because of the low predictive value and misclassification of the

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

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    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.

  11. Activity screening of plant growth promoting rhizobacteria isolated from alfalfa rhizosphere

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    shahla pashapour

    2016-03-01

    Full Text Available 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 rhizosphere and root nodules grown around Zanjan. Materials and methods: These bacteria were isolated from alfalfa roots grown around Zinc industries in Zanjan province. After bacterial isolation and purification from root and soil samples, isolates were screened in vitro for plant growth promoting traits such as IAA (Indole Acetic Acid, ACC- deaminase (Amino Cyclopropan Carboxylate, HCN (Hydrogen Cyanide, siderophore, chitinase production and mineral and organic phosphate solubilization activities. Results: The results indicated that 43 bacterial isolates produced IAA (4.04- 4.95 μg/ml and 15 isolates produced ACC- deaminase (0.23- 1.05 μg/ml. Only one isolate (Rm66 produced high amount of HCN. Qualitative siderophore production was observed in 9 isolates. None of the isolates produced chitinase. Solubilization of mineral phosphate was commonly detected in 19 isolates (4.33- 5.86 μg/ml, and 15 isolates solubilized organic phosphate (1.66- 144.28 μg/ml. Discussion and conclusion: This study shows that most of the bacterial strains which isolated from alfalfa cultivated lands had PGP activities and also a good potential to increase plant growth after inoculation with to seeds as eco- friendly fertilizers.

  12. Yield of active screening for tuberculosis among asylum seekers in Germany: a systematic review and meta-analysis.

    Science.gov (United States)

    Bozorgmehr, Kayvan; Razum, Oliver; Saure, Daniel; Joggerst, Brigitte; Szecsenyi, Joachim; Stock, Christian

    2017-03-23

    All asylum seekers in Germany undergo upon-entry screening for tuberculosis TB, but comprehensive evidence on the yield is lacking. We compared the national estimates with the international literature in a systematic review and meta-analysis of studies reporting the yield of TB, defined as the fraction of active TB cases detected among asylum seekers screened in Germany upon entry. We searched 11 national and international databases for empirical studies and the internet for grey literature published in English or German without restrictions on publication time. Among 1,253 screened articles, we identified six articles reporting the yield of active TB based on German data, ranging from 0.72 (95% confidence interval (CI): 0.45-1.10) to 6.41 (95% CI: 4.19-9.37) per 1,000 asylum seekers. The pooled estimate across all studies was 3.47 (95% CI: 1.78-5.73; I 2  = 94.9%; p asylum seekers. This estimate was in line with international evidence (I 2  = 0%; p for heterogeneity 0.55). The meta-analysis of available international estimates resulted in a pooled yield of 3.04 (95% CI: 2.24-3.96) per 1,000. This study provides an estimate across several German federal states for the yield of TB screening in asylum seekers. Further research is needed to develop more targeted screening programmes. This article is copyright of The Authors, 2017.

  13. Screening for Proteolytic Activities in Snake Venom by Means of a Multiplexing ESI-MS Assay Scheme

    NARCIS (Netherlands)

    Liesener, A.; Perchuc, Anna-Maria; Schöni, Reto; Wilmer, Marianne; Karst, U.

    2005-01-01

    A multiplexed mass spectrometry based assay scheme for the simultaneous determination of five different substrate/product pairs was developed as a tool for screening of proteolytic activities in snake venom fractions from Bothrops moojeni. The assay scheme was employed in the functional

  14. Is the association between screen-based behaviour and health complaints among adolescents moderated by physical activity?

    NARCIS (Netherlands)

    Brindova, Daniela; Veselska, Zuzana Dankulincova; Klein, Daniel; Hamrik, Zdenek; Sigmundova, Dagmar; van Dijk, Jitse P.; Reijneveld, Sijmen A.; Geckova, Andrea Madarasova

    OBJECTIVES: The aim of this study was to assess the association between screen-based (SB) behaviour and selected health complaints in adolescents and whether physical activity (PA) moderates this association. METHODS: Data from the cross-sectional Health Behaviour of School-aged Children study

  15. Development of inhibitors of the 2C-methyl-D-erythritol 4-phosphate (MEP) pathway enzymes as potential anti-infective agents.

    Science.gov (United States)

    Masini, Tiziana; Hirsch, Anna K H

    2014-12-11

    Important pathogens such as Mycobacterium tuberculosis and Plasmodium falciparum, the causative agents of tuberculosis and malaria, respectively, and plants, utilize the 2C-methyl-D-erythritol 4-phosphate (MEP, 5) pathway for the biosynthesis of isopentenyl diphosphate (1) and dimethylallyl diphosphate (2), the universal precursors of isoprenoids, while humans exclusively utilize the alternative mevalonate pathway for the synthesis of 1 and 2. This distinct distribution, together with the fact that the MEP pathway is essential in numerous organisms, makes the enzymes of the MEP pathway attractive drug targets for the development of anti-infective agents and herbicides. Herein, we review the inhibitors reported over the past 2 years, in the context of the most important older developments and with a particular focus on the results obtained against enzymes of pathogenic organisms. We will also discuss new discoveries in terms of structural and mechanistic features, which can help to guide a rational development of inhibitors.

  16. Effect of sputum suction by bronchofiberoscope combined with routine anti-infective therapy on lung function and inflammatory state in patients with severe lung infection

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    Jian Sun

    2016-07-01

    Full Text Available Objective: To analyze the effect of sputum suction by bronchofiberoscope combined with routine anti-infective therapy on lung function and inflammatory state in patients with severe lung infection. Methods: A total of 52 patients with severe lung infection who received treatment in our hospital from January 2015 to December 2015 were selected as research subjects and were divided into observation group 26 cases and control group 26 cases according to different treatment methods. Differences in levels of lung function indexes, serum inflammation-related factors, disease severity-related indexes, JNK/SAPK and TLR2/NF-κB signaling pathways were compared between two groups. Results: FEV1, MMV, MMEF, FRC and TLC values of observation group after treatment were higher than those of control group (P<0.05; serum PAF, MIP-1毩, sTREM-1 and PCT values of observation group were lower than those of control group while APN value was higher than that of control group (P<0.05; serum ACE, NO, ET-1, SP-A and HMGB1 values of observation group were lower than those of control group while CC16 and ChE values were higher than those of control group (P<0.05; JNK, SAPK, TLR2 and NF-κB protein expression levels of observation group were lower than those of control group (P<0.05. Conclusions: Sputum suction by bronchofiberoscope combined with routine anti-infective therapy for patients with severe lung infection has positive significance in improving patients’ lung function, inhibiting systemic inflammation and other aspects.

  17. Evidence for the hERG Liability of Antihistamines, Antipsychotics, and Anti-Infective Agents: A Systematic Literature Review From the ARITMO Project.

    Science.gov (United States)

    Hazell, Lorna; Raschi, Emanuel; De Ponti, Fabrizio; Thomas, Simon H L; Salvo, Francesco; Ahlberg Helgee, Ernst; Boyer, Scott; Sturkenboom, Miriam; Shakir, Saad

    2017-05-01

    A systematic review was performed to categorize the hERG (human ether-a-go-go-related gene) liability of antihistamines, antipsychotics, and anti-infectives and to compare it with current clinical risk of torsade de pointes (TdP). Eligible studies were hERG assays reporting half-minimal inhibitory concentrations (IC50). A "hERG safety margin" was calculated from the IC50 divided by the peak human plasma concentration (free C max ). A margin below 30 defined hERG liability. Each drug was assigned an "uncertainty score" based on volume, consistency, precision, and internal and external validity of evidence. The hERG liability was compared to existing knowledge on TdP risk (www.credibledrugs.org). Of 1828 studies, 82 were eligible, allowing calculation of safety margins for 61 drugs. Thirty-one drugs (51%) had evidence of hERG liability including 6 with no previous mention of TdP risk (eg, desloratadine, lopinavir). Conversely, 16 drugs (26%) had no evidence of hERG liability including 6 with known, or at least conditional or possible, TdP risk (eg, chlorpromazine, sulpiride). The main sources of uncertainty were the validity of the experimental conditions used (antihistamines and antipsychotics) and nonuse of reference compounds (anti-infectives). In summary, hERG liability was categorized for 3 widely used drug classes, incorporating a qualitative assessment of the strength of available evidence. Some concordance with TdP risk was observed, although several drugs had hERG liability without evidence of clinical risk and vice versa. This may be due to gaps in clinical evidence, limitations of hERG/C max data, or other patient/drug-specific factors that contribute to real-life TdP risk. © 2016, The American College of Clinical Pharmacology.

  18. 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.

  19. Antioxidant activity and phytochemical screening of two Cucurbitaceae: Citrullus colocynthis fruits and Bryonia dioica roots

    Directory of Open Access Journals (Sweden)

    Echaimaa Chekroun

    2015-08-01

    Full Text Available Objective: To evaluate antioxidant activity and quantify total content of polyphenols and flavonoids in two Cucurbitaceae plant extracts, Citrullus colocynthis (C. colocynthis fruits and Bryonia dioica (B. dioica roots. Methods: Qualitative and quantitative analysis of aqueous and butanolic extracts, prepared from C. colocynthis fruits and B. dioica roots was carried out using standard methods. Estimation of their antioxidant activity was determined by free radical scavenging activity assay using 2,2-diphenyl-l-picrylhydrazyl and ferric reducing antioxidant power assay. Results: Preliminary phytochemical screening of the aqueous and organic extracts showed the presence of tannins, flavanoids, terpenoids, saponins and quinones. The content of phenolic compounds varies among the two species of cucurbits and even in the different extracts of the same species. The most important amount of total polyphenols and flavanoids expressed respectively as gallic acid and catechin equivalent per gram extract, was determined in butanolic extract of B. dioica roots (541.78 mg/g, 120.60 mg/g. The lowest values were noted in C. colocynthis fruit aqueous extract (219.58 mg/g, 46.13 mg/g. Butanolic extract of B. dioica roots exhibited an interesting free radical scavenging activity with IC50 = 2.25 µg/mL compared to IC50 = 1.5 µg/mL of ascorbic acid, followed by B. dioica roots aqueous extract (IC50 = 47.25 µg/mL, butanolic C. colocynthis fruit extract (IC50 = 61 µg/mL and C. colocynthis fruit aqueous extract (IC50 = 241.25 µg/mL. A highest reducing power was observed in B. dioica roots butanolic extract compared to other extracts (C. colocynthis fruit aqueous and butanolic extracts and B. dioica roots aqueous extract. Conclusions: The results indicate that the wealth of B. dioica roots extracts on polyphenols and flavonoids is more than C. colocynthis fruit extracts. These phytoconstituents ensure an interesting free radical scavenging activity and reducing

  20. Antioxidant activity and phytochemical screening of the methanol extracts of Euphorbia hirta L.

    Science.gov (United States)

    Basma, Abu Arra; Zakaria, Zuraini; Latha, Lacimanan Yoga; Sasidharan, Sreenivasan

    2011-05-01

    To assess antioxidant activities of different parts of Euphorbia hirta (E. hirta), and to search for new sources of safe and inexpensive antioxidants. Samples of leaves, stems, flowers and roots from E. hirta were tested for total phenolic content, and flavonoids content and in vitro antioxidant activity by diphenyl-1-picrylhydrazyl (DPPH) assay and reducing power was measured using cyanoferrate method. The leaves extract exhibited a maximum DPPH scavenging activity of (72.96±0.78)% followed by the flowers, roots and stems whose scavenging activities were (52.45±0.66)%, (48.59±0.97)%, and (44.42±0.94)%, respectively. The standard butylated hydroxytoluene (BHT) was (75.13±0.75)%. The IC(50) for leaves, flowers, roots, stems and BHT were 0.803, 0.972, 0.989, 1.358 and 0.794 mg/mL, respectively. The reducing power of the leaves extract was comparable with that of ascorbic acid and found to be dose dependent. Leaves extract had the highest total phenolic content [(206.17±1.95) mg GAE/g], followed by flowers, roots and stems extracts which were (117.08±3.10) mg GAE/g, (83.15±1.19) mg GAE/g, and (65.70±1.72) mg GAE/g, respectively. On the other hand, total flavonoids content also from leave had the highest value [(37.970±0.003) mg CEQ/g], followed by flowers, roots and stems extracts which were (35.200±0.002) mg CEQ/g, (24.350±0.006) mg CEQ/g, and (24.120±0.004) mg CEQ/g, respectively. HPTLC bioautography analysis of phenolic and antioxidant substance revealed phenolic compounds. Phytochemical screening of E. hirta leaf extract revealed the presence of reducing sugars, terpenoids, alkaloids, steroids, tannins, flavanoids and phenolic compounds. These results suggeste that E. hirta have strong antioxidant potential. Further study is necessary for isolation and characterization of the active antioxidant agents, which can be used to treat various oxidative stress-related diseases. Copyright © 2011 Hainan Medical College. Published by Elsevier B.V. All rights

  1. Screening Cellulose Activity of Yeast Isolated from Soil, Sediment and Water River from Taman Nasional Gunung Halimun, West Java, Indonesia

    Directory of Open Access Journals (Sweden)

    Mangunwardoyo, W.

    2011-01-01

    Full Text Available A total of 245 yeast isolates from Gunung Halimun National Park (GHNP were screened for cellulolytic activity using 0.2% cellulose-azure. The results showed that 16 isolates have cellulolytic activity using cellulose-azure assay. These isolates were further screened for carboxymethyl cellulase (CMCase, avicelase and cellobiase using specific substrates (carboxymethyl cellulosa, avicel and cellobiose with Teather and Wood method. The results showed that 7 isolates have CMCase; 6 isolates have cellobiase; 2 isolates have CMCase and cellobiase; and 1 isolate has CMCase and avicelase and cellobiase activities. Isolate S 4121 has the highest CMCase activity and identified as Trichosporon sporotrichoides (van Oorschot van Oorschot and de Hoog UICC Y-286.

  2. 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.

  3. A cell-based, high content screening assay reveals activators and inhibitors of cancer cell invasion

    Science.gov (United States)

    Quintavalle, Manuela; Elia, Leonardo; Price, Jeffrey H.; Heynen-Genel, Susanne; Courtneidge, Sara A.

    2012-01-01

    Acquisition of invasive cell behavior underlies tumor progression and metastasis. To define in more molecular detail the mechanisms underlying invasive behavior, we developed a high throughput screening strategy to quantitate invadopodia; actin-rich membrane protrusions of cancer cells which contribute to tissue invasion and matrix remodeling. We developed a high content, imaged-based assay, and tested the LOPAC 1280 collection of pharmacologically active agents. We found compounds that potently inhibited invadopodia formation without overt toxicity, as well as compounds that increased invadopodia number. One of the two compounds that increased both invadopodia number and invasive behavior was the chemotherapeutic agent paclitaxel, which has potential clinical implications for its use in the neoadjuvant and resistance settings. Several of the invasion inhibitors were annotated as cyclin-dependent kinase (cdk) inhibitors. Loss-of-function experiments determined that Cdk5 was the relevant target. We further determined that the mechanism by which Cdk5 promotes both invadopodia formation and cancer invasion is by phosphorylation and down regulation of the actin regulatory protein caldesmon. PMID:21791703

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

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    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.

  5. Screening of common Plantago species in Hungary for bioactive molecules and antioxidant activity.

    Science.gov (United States)

    Gonda, S; Tóth, L; Parizsa, P; Nyitrai, M; Vasas, G

    2010-01-01

    Five species of Plantago genus, namely P. lanceolata, P. major, P. media, P. altissima and P. maritima were screened for iridoid content (CE-MEKC), total caffeoyl phenylethanoid glycoside (CPG) content and antioxidant activity (CUPRAC assay). The five species could be distinguished by TLC pattern analysis in a single run in a system commonly used for quality management of P. lanceolata leaves, as shown by cluster analysis of major bands; with the exception, that P. altissima and P. lanceolata did not show enough pattern difference to be fully separated. P. maritima was shown to have the highest antioxidant capacity (0.42 μmol ascorbic acid equivalent (AAE)/g DW), and the highest level of CPGs (4.29%). P. altissima was shown to be chemically indistinguishable from P. lanceolata with repsect to iridoid content (aucubin 0.55 ± 0.04%, 0.68 ± 0.23%, catalpol 0.66 ± 0.13% and 0.89 ± 0.22%, respectively), CPG content (2.40 ± 0.38% and 2.54 ± 0.56%, respectively) and antioxidant capacity (0.2206 ± 0.0290 and 0.2428 ± 0.0191 μmol AAEAC/g DW). The presented data show the potency of medicinal use of Hungarian wild populations of the studied five species, especially in the case of P. maritima, and that P. altissima can be a potential replacement of P. lanceolata in herbal mixtures.

  6. A pilot of a video game (DDR) to promote physical activity and decrease sedentary screen time.

    Science.gov (United States)

    Maloney, Ann E; Bethea, T Carter; Kelsey, Kristine S; Marks, Julie T; Paez, Sadye; Rosenberg, Angela M; Catellier, Diane J; Hamer, Robert M; Sikich, Linmarie

    2008-09-01

    We examined the feasibility of Dance Dance Revolution (DDR), a dance video game, in participants' homes, to increase physical activity (PA) and to decrease sedentary screen time (SST). Sixty children (7.5 +/- 0.5 years) were randomized in a 2:1 ratio to DDR or to wait-list control (10-week delay). DDR use was logged, PA was measured objectively by accelerometry. SST was self-reported at weeks 0 and 10. At week 28, after both groups had access to DDR, accelerometry and SST were repeated. Mean use of DDR was 89 +/- 82 (range 0-660 min) min per week (mpw). The DDR group showed increased vigorous PA and a reduction in light PA; the control group showed no increase in moderate and/or vigorous PA (MVPA) although they also had a reduction in light PA. Differences between the groups were not observed. The DDR group also reported a decrease in SST of -1.2 +/- 3.7 h per week (hpw) (P DDR group. Between weeks 10 and 28, numeric reductions in SST were reported in both groups. In the DDR group, SST at week 28 (8.8 +/- 6.0 hpw) was lower than baseline (10.5 +/- 5.5 hpw; P DDR reduces SST and may facilitate slight increases in vigorous PA. Further study is needed to better characterize children and contexts in which DDR may promote a healthy lifestyle.

  7. Fluorometric method for inorganic pyrophosphatase activity detection and inhibitor screening based on click chemistry.

    Science.gov (United States)

    Xu, Kefeng; Chen, Zhonghui; Zhou, Ling; Zheng, Ou; Wu, Xiaoping; Guo, Longhua; Qiu, Bin; Lin, Zhenyu; Chen, Guonan

    2015-01-06

    A fluorometric method for pyrophosphatase (PPase) activity detection was developed based on click chemistry. Cu(II) can coordinate with pyrophosphate (PPi), the addition of pyrophosphatase (PPase) into the above system can destroy the coordinate compound because PPase catalyzes the hydrolysis of PPi into inorganic phosphate and produces free Cu(II), and free Cu(II) can be reduced by sodium ascorbate (SA) to form Cu(I), which in turn initiates the ligating reaction between nonfluorescent 3-azidocoumarins and terminal alkynes to produce a highly fluorescent triazole complex, based on which, a simple and sensitive turn on fluorometric method for PPase can be developed. The fluorescence intensity of the system has a linear relationship with the logarithm of the PPase concentration in the range of 0.5 and 10 mU with a detection limit down to 0.2 mU (S/N = 3). This method is cost-effective and convenient without any labels or complicated operations. The proposed system was applied to screen the potential PPase inhibitor with high efficiency. The proposed method can be applied to diagnosis of PPase-related diseases.

  8. 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.

  9. 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.

  10. Preliminary phytochemical screening and in vitro antibacterial activity of Bauhinia variegata Linn. against human pathogens

    Directory of Open Access Journals (Sweden)

    Sonam Pandey

    2015-02-01

    Full Text Available Objective: To investigate the antimicrobial and phytochemical properties of hydromethanolic extracts of Bauhinia variegata Linn. (B. variegata (leaf, stem bark and flower to justify the traditional claim endowed upon this herbal drug as a rasayana in Ayurveda. This study thus can be further utilized to formulate the natural antioxidant which can be used as a dietary supplement to fight against several diseases such as cancer, ageing, arthrosclerosis, etc. Methods: The study showed that the number of different phytoconstituents present in the plant which makes it remarkable for its use by traditional practitioners. On the another set of experiment, the hydromethanolic extract of B. variegata (leaf, stem bark and flower were evaluated against Gram-positive and Gram-negative by using disk diffusion assay. Results: Phytochemical screening of all extracts showed the presence of alkaloids, steroids, phenolic compounds, tannins, saponin, carbohydrates, proteins, amino acids and organic acids. The antibacterial activity of all the extracts (leaf, stem bark and flower of B. variegata was determined by agar well diffusion method at four different concentrations i.e., 1 000 mg/mL, 750 mg/mL, 500 mg/mL and 250 mg/mL using Gram-positive Bacillus subtilius, Staphylococcus aureus and Streptococcus epidermidis and Gram-negative Escherichia coli, Shegilla flexineria, Pseudomonas auriginosa bacteria. Conclusions: These studies show that hydromethanolic extracts of B. variegata (leaf, stem bark and flower inhibited the growth of microorganism ’s in dose dependently. B. variegata leaf, stem bark and flower extracts have several phytochemical constituents who possess the antimicrobial activity. A tiny amount of data is presented, as the preliminary antimicrobial properties of the B. variegata here accessed, under the urgent necessity of new antibiotics in the market and in face of the increased resistance of infectious microorganisms to antimicrobials.

  11. Phytochemical screening and biological activities of trigonella incisa and nonea edgeworthii

    International Nuclear Information System (INIS)

    Rehman, S.; Ahmad, N.; Shinwari, Z.K.; Ahmad, I.

    2017-01-01

    The extracts and its derived fractions from two important medicinal plants species Trigonella incisa and Nonea edgeworthii were tested for biochemical potential. The aim of our research was to encourage drug finding work with plants. The crude extract and fractions from Trigonella incisa plant were found to be most potent against Pseudomonas aeuriginosa as compared to Escherichia coli and Salmonella typhi. The Chloroform fraction showed outstanding inhibition 11 mm against Pseudomonas aeuriginosa followed by crude extract, n-butanol and aqueous fractions each giving 9 mm inhibition. The n-butanol fraction of Trigonella incisa revealed 8 mm inhibition against Escherichia coli second by aqueous fraction with 7 mm inhibition. Moderate inhibition (8 mm) was showed by crude extract and chloroform fraction against Salmonella typhi. In case of Nonea edgeworthii plant aqueous and ethyl acetate fraction were found to be most active against Pseudomonas aeuriginosa and Escherichia coli giving inhibition of 14 mm each which is found to be best inhibition even more than the inhibition showed by antibiotic used. Crude extract and chloroform fraction of the plant showed 12 mm and 10 mm inhibition against Salmonella typhi. Both the selected plants were found equally potential against the tested fungi. n-hexane and chloroform fractions of Trigonella incisa give 10 mm inhibition against Fusarium oxysporum and Alternaria alternata respectively while crude extract from Nonea edgeworthii give 11 mm inhibition against Alternaria alternata. Over all poor scavenging activity was showed by selected plants. Ethyl acetate fraction of both plants was found to be reasonably good when compared with standard. The low antioxidant profile of the plants may be due to the absence of flavonoids in plants .In preliminary phytochemical screening alkaloid, phenol and saponins were reported in both plants. (author)

  12. High-throughput screening and whole genome sequencing identifies an antimicrobially active inhibitor of Vibrio cholerae.

    Science.gov (United States)

    Sergeev, Galina; Roy, Sambit; Jarek, Michael; Zapolskii, Viktor; Kaufmann, Dieter E; Nandy, Ranjan K; Tegge, Werner

    2014-02-26

    Pathogenic serotypes of Vibrio cholerae cause the life-threatening diarrheal disease cholera. The increasing development of bacterial resistances against the known antibiotics necessitates the search for new antimicrobial compounds and targets for this pathogen. A high-throughput screening assay with a Vibrio cholerae reporter strain constitutively expressing green fluorescent protein (GFP) was developed and applied in the investigation of the growth inhibitory effect of approximately 28,300 structurally diverse natural compounds and synthetic small molecules. Several compounds with activities in the low micromolar concentration range were identified. The most active structure, designated vz0825, displayed a minimal inhibitory concentration (MIC) of 1.6 μM and a minimal bactericidal concentration (MBC) of 3.2 μM against several strains of V. cholerae and was specific for this pathogen. Mutants with reduced sensitivity against vz0825 were generated and whole genome sequencing of 15 pooled mutants was carried out. Comparison with the genome of the wild type strain identified the gene VC_A0531 (GenBank: AE003853.1) as the major site of single nucleotide polymorphisms in the resistant mutants. VC_A0531 is located on the small chromosome of V. cholerae and encodes the osmosensitive K+-channel sensor histidine kinase (KdpD). Nucleotide exchange of the major mutation site in the wild type strain confirmed the sensitive phenotype. The reporter strain MO10 pG13 was successfully used for the identification of new antibacterial compounds against V. cholerae. Generation of resistant mutants and whole genome sequencing was carried out to identify the histidine kinase KdpD as a novel antimicrobial target.

  13. Perceived neighborhood safety related to physical activity but not recreational screen-based sedentary behavior in adolescents.

    Science.gov (United States)

    Lenhart, Clare M; Wiemken, Andrew; Hanlon, Alexandra; Perkett, Mackenzie; Patterson, Freda

    2017-09-18

    A growing proportion of adolescents have poor cardiovascular health behaviors, including low levels of physical activity and high levels of sedentary behavior, thus increasing the likelihood of poor heart health in later years. This study tested the hypothesis that low perceived neighborhood safety would be associated with low levels of physical activity and high levels of recreational sedentary behavior in high-school students. Using cross-sectional, weighted data from the 2015 Pennsylvania (USA) State and Philadelphia city Youth Risk Behavior Survey, multivariable logistic regression modeling was used to examine the association between perceived neighborhood safety, and physical activity levels and recreational screen-based sedentary behavior time respectively, while controlling for potential confounders. After adjustment for other significant correlates of physical activity, students with low perceived neighborhood safety had a 21% reduced odds of being physically active on 5 or more days of the last week as compared to those who felt safe (p = 0.044). Perceived safety was not related to sedentary behavior; but sports team participation emerged as a strong correlate of low screen-based sedentary behavior (OR = 0.73, p = .002). These data add to a growing body of work demonstrating the importance of perceived safety with physical activity levels in youth. Sports team participation may be a viable target to reduce screen-based sedentary time.

  14. Perceived neighborhood safety related to physical activity but not recreational screen-based sedentary behavior in adolescents

    Directory of Open Access Journals (Sweden)

    Clare M. Lenhart

    2017-09-01

    Full Text Available Abstract Background A growing proportion of adolescents have poor cardiovascular health behaviors, including low levels of physical activity and high levels of sedentary behavior, thus increasing the likelihood of poor heart health in later years. This study tested the hypothesis that low perceived neighborhood safety would be associated with low levels of physical activity and high levels of recreational sedentary behavior in high-school students. Methods Using cross-sectional, weighted data from the 2015 Pennsylvania (USA State and Philadelphia city Youth Risk Behavior Survey, multivariable logistic regression modeling was used to examine the association between perceived neighborhood safety, and physical activity levels and recreational screen-based sedentary behavior time respectively, while controlling for potential confounders. Results After adjustment for other significant correlates of physical activity, students with low perceived neighborhood safety had a 21% reduced odds of being physically active on 5 or more days of the last week as compared to those who felt safe (p = 0.044. Perceived safety was not related to sedentary behavior; but sports team participation emerged as a strong correlate of low screen-based sedentary behavior (OR = 0.73, p = .002. Conclusion These data add to a growing body of work demonstrating the importance of perceived safety with physical activity levels in youth. Sports team participation may be a viable target to reduce screen-based sedentary time.

  15. Impact of x-ray screening programmes for active tuberculosis in homeless populations: a systematic review of original studies.

    Science.gov (United States)

    Curtis, Jonathan

    2016-03-01

    Tuberculosis prevalence is generally low in industrialized countries, but many cities now operate surveillance programmes to actively screen for tuberculosis in known risk groups including homeless people. While several studies have reported on individual screening programmes, this study is the first known systematic review specifically looking at chest x-ray screening programmes for tuberculosis in homeless populations. Systematic review of relevant studies published in the last 20 years using the PRISMA checklist. Fourteen studies were reviewed: 12 cross-sectional studies, 1 retrospective cohort study and 1 'data-linkage' study. The studies were heterogenous in terms of the objectives, measured outcomes and methodological quality. Active tuberculosis prevalence was found to be higher in homeless populations and screening programmes appear to identify tuberculosis earlier, reduce prevalence and transmission, and increase treatment compliance. Active x-ray surveillance programmes in homeless communities appear to be cost-effective in reducing prevalence within the homeless population particularly in related strains and may have some benefits over passive finding. While there is a need for high-quality research to further assess the impact of these programmes, this study has outlined the benefits and limitations of existing programmes and included recommendations to achieve maximum coverage, uptake and cost-benefit. © The Author 2015. Published by Oxford University Press on behalf of Faculty of Public Health. All rights reserved. For permissions, please e-mail: journals.permissions@oup.com.

  16. Physical activity and screen time in adolescents in the chronic kidney disease in children (CKiD) cohort.

    Science.gov (United States)

    Clark, Stephanie L; Denburg, Michelle R; Furth, Susan L

    2016-05-01

    Self-reported physical activity (PA) and screen time exposure in adolescents with chronic kidney disease (CKD) has not been evaluated. We performed a cross-sectional analysis of PA and screen time in 224 adolescents at entry into the Chronic Kidney Disease in Children (CKiD) cohort. We compared proportions of CKiD vs. healthy 2012 National Health and Nutrition Examination Survey (NHANES) participants reporting the recommended 60 min of PA 7 days/week or ≤ 2 h/day of entertainment screen time (binomial probability test). Within CKiD, we assessed correlates of PA and screen time using multivariable logistic and linear regression and examined longitudinal data for 136 participants. Median age of CKiD participants was 15 years, and 60 % were male. Median estimated glomerular filtration rate (eGFR) was 41.3 (IQR 30.8, 52.3) ml/min/1.73 m(2). Only 13 % of CKiD participants met recommendations for PA vs. 25 % of NHANES (p < 0.001), while 98 % in CKiD exceeded the recommended screen time vs. 73 % in NHANES (p < 0.001). Within CKiD, obesity (p = 0.04) and lower eGFR (p = 0.02) were independently associated with greater screen time. Adolescents with CKD engage in significantly less PA and greater screen time than healthy youth in the United States, and this may worsen over time.

  17. 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.

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

    Directory of Open Access Journals (Sweden)

    Michael Russelle Alvarez

    2016-02-01

    Full Text Available 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.

  19. Do school physical activity policies and programs have a role in decreasing multiple screen time behaviours among youth?

    Science.gov (United States)

    Katapally, Tarun R; Laxer, Rachel E; Qian, Wei; Leatherdale, Scott T

    2018-05-01

    Screen time in youth has been associated with a wide range of poor health outcomes. Evidence indicates the need to develop physical activity (PA) school policies and programs that are aimed at decreasing youth screen time behaviours. This study aims to understand the association between PA policies and programs embedded into the functioning of 89 schools across two provinces in Canada and multiple screen time behaviours. As part of the COMPASS Study, a total of 44,861 youth aged between 13 and 18years and belonging to 89 schools in two Canadian provinces completed a validated questionnaire for health behaviours and outcomes data. PA policies and programs were measured using the School Policies and Practices Questionnaire, completed by the relevant school administrator. Participation in before-school, noon hour, or after-school intramural programs, participation in varsity sports, and access to indoor areas of PA during non-instructional time, was associated with significantly lower multiple screen time behaviours across both provinces. With exposure to multiple electronic and digital devices only predicted to increase among youth in the future, there is a need to conceptualize and integrate school-based screen time reducing PA policies and programs into the regular functioning of the schools. Copyright © 2017 Elsevier Inc. All rights reserved.

  20. Pre-meal screen-time activities increase subjective emotions, but not food intake in young girls.

    Science.gov (United States)

    Totosy de Zepetnek, Julia O; Pollard, Damion; Welch, Jo M; Rossiter, Melissa; Faghih, Shiva; Bellissimo, Nick

    2017-04-01

    To determine the effect of pre-meal screen-time activities on subjective emotions, subjective appetite, and food intake (FI) in 9-14 year-old girls. In this clinical study, 31 girls completed four 45-min treatment conditions of television viewing (TVV), video game playing (VGP), a challenging computer task (CT), and sitting without screen exposure (control) in a randomized order. Each treatment condition was followed immediately by an ad libitum pizza lunch, and FI was calculated from the weight of the consumed pizza. Subjective appetite was assessed at baseline, 15, 30, and 45 min during the treatment condition, and upon trial completion at 75 min. Subjective emotions were assessed at baseline and at 45 min. FI was not affected by screen type, but was positively correlated with body composition (fat mass [FM, kg], fat free mass [FFM, kg]) in all treatment conditions. Subjective appetite was not affected by screen type, but increased with time in all treatment conditions (p emotions were affected by VGP only. Anger, excitement, frustration, and upset feelings were increased at 45 min following VGP. VGP led to increased frustration compared to control (p = 0.0003), CT (p = 0.007) and TVV (p = 0.0002). Exposure to TVV or CT before eating did not affect subjective emotions, subjective appetite, or FI, and no difference was found between screen activities and the control condition for average appetite or FI. Despite a change in subjective emotions during the VGP condition, there was no increase in subjective appetite or subsequent FI. These findings suggest that physiologic signals of satiation and satiety are not overridden by environmental stimuli of pre-meal screen-time exposure among young girls. (Clinical trial number NCT01750177). Copyright © 2016 Elsevier Ltd. All rights reserved.

  1. 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

    2007-03-01

    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.

  2. Cell-based screening assay for anti-inflammatory activity of bioactive compounds

    NARCIS (Netherlands)

    Meijer, Kees; Vonk, Roel J.; Priebe, Marion G.; Roelofsen, Han

    2015-01-01

    Excess dietary intake may induce metabolic inflammation which is associated with insulin resistance and cardiovascular disease. Recent evidence indicates that dietary bioactive compounds may diminish metabolic inflammation. To identify anti-inflammatory bioactives, we developed a screening assay

  3. Screening for the presence of antimicrobial activity in few Indian seaweeds

    Digital Repository Service at National Institute of Oceanography (India)

    Kotnala, S.; Garg, Aakriti; Chatterji, A.

    found to be a novel source of cytotoxic; whereas penta, halogenated monoterpene, halomon, exhibit one of the most extreme examples of differential cytotoxicity in the screening conducted by the National Cancer Institute (NCI), USA. In specific...

  4. Cross-sectional associations between maternal parenting styles, physical activity and screen sedentary time in children.

    Science.gov (United States)

    Van der Geest, K E; Mérelle, S Y M; Rodenburg, G; Van de Mheen, D; Renders, C M

    2017-09-29

    Children's activity level, including physical activity (PA) and screen sedentary time (SST), is influenced by environmental factors in which parents play a critical role. Different types of parenting styles may influence children's activity level. Inconsistent results were found on the association between parenting styles and PA, and few studies tested the association between parenting styles and SST. This study examined the association between parenting styles, PA and SST and the modifying effect of children's gender and maternal educational level on these associations. Cross-sectional data were collected from parents of children aged 8-11 years old who completed a web-based non-standardized questionnaire (N = 4047). Since 85% of the questionnaires were filled in by mothers, parenting styles are mainly reported by mothers. Multiple linear regression techniques were used to assess the associations between parenting styles (authoritative, permissive, authoritarian and neglectful), and PA and SST (mean min/day). The modifying effect of children's gender and maternal educational level on these associations was explored. P values ≤.0125 were considered as statistically significant based on the Bonferroni correction for four primary analyses. The neglectful parenting style was most widely used (35.3%), while the authoritarian style was least common (14.8%). No significant association was found between parenting styles and PA level. As regards SST, an authoritative parenting style was significantly associated with lower SST in boys while a neglectful parenting style was significantly associated with higher SST in both boys and girls. When the mother had a medium educational level, an authoritative parenting style was significantly associated with lower SST while neglectful parenting was significantly associated with higher SST. No association was found between parenting styles and PA. However, an authoritative parenting style was associated with a reduction in SST

  5. Cross-sectional associations between maternal parenting styles, physical activity and screen sedentary time in children

    Directory of Open Access Journals (Sweden)

    K. E. Van der Geest

    2017-09-01

    Full Text Available Abstract Background Children’s activity level, including physical activity (PA and screen sedentary time (SST, is influenced by environmental factors in which parents play a critical role. Different types of parenting styles may influence children’s activity level. Inconsistent results were found on the association between parenting styles and PA, and few studies tested the association between parenting styles and SST. This study examined the association between parenting styles, PA and SST and the modifying effect of children’s gender and maternal educational level on these associations. Methods Cross-sectional data were collected from parents of children aged 8–11 years old who completed a web-based non-standardized questionnaire (N = 4047. Since 85% of the questionnaires were filled in by mothers, parenting styles are mainly reported by mothers. Multiple linear regression techniques were used to assess the associations between parenting styles (authoritative, permissive, authoritarian and neglectful, and PA and SST (mean min/day. The modifying effect of children’s gender and maternal educational level on these associations was explored. P values ≤.0125 were considered as statistically significant based on the Bonferroni correction for four primary analyses. Results The neglectful parenting style was most widely used (35.3%, while the authoritarian style was least common (14.8%. No significant association was found between parenting styles and PA level. As regards SST, an authoritative parenting style was significantly associated with lower SST in boys while a neglectful parenting style was significantly associated with higher SST in both boys and girls. When the mother had a medium educational level, an authoritative parenting style was significantly associated with lower SST while neglectful parenting was significantly associated with higher SST. Conclusions No association was found between parenting styles and PA. However, an

  6. Novel Data Mining Methods for Virtual Screening of Biological Active Chemical Compounds

    KAUST Repository

    Soufan, Othman M.

    2016-11-23

    Drug discovery is a process that takes many years and hundreds of millions of dollars to reveal a confident conclusion about a specific treatment. Part of this sophisticated process is based on preliminary investigations to suggest a set of chemical compounds as candidate drugs for the treatment. Computational resources have been playing a significant role in this part through a step known as virtual screening. From a data mining perspective, availability of rich data resources is key in training prediction models. Yet, the difficulties imposed by big expansion in data and its dimensionality are inevitable. In this thesis, I address the main challenges that come when data mining techniques are used for virtual screening. In order to achieve an efficient virtual screening using data mining, I start by addressing the problem of feature selection and provide analysis of best ways to describe a chemical compound for an enhanced screening performance. High-throughput screening (HTS) assays data used for virtual screening are characterized by a great class imbalance. To handle this problem of class imbalance, I suggest using a novel algorithm called DRAMOTE to narrow down promising candidate chemicals aimed at interaction with specific molecular targets before they are experimentally evaluated. Existing works are mostly proposed for small-scale virtual screening based on making use of few thousands of interactions. Thus, I propose enabling large-scale (or big) virtual screening through learning millions of interaction while exploiting any relevant dependency for a better accuracy. A novel solution called DRABAL that incorporates structure learning of a Bayesian Network as a step to model dependency between the HTS assays, is showed to achieve significant improvements over existing state-of-the-art approaches.

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

    Science.gov (United States)

    Feng, Qi; Zhang, Qing-le; Du, Yue; Ye, Yong-ling; He, Qi-qiang

    2014-01-01

    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.

  8. 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.

  9. Screening of north-east Mexico medicinal plants with activities against herpes simplex virus and human cancer cell line.

    Science.gov (United States)

    Silva-Mares, David; Rivas-Galindo, Veronica M; Salazar-Aranda, Ricardo; Pérez-Lopez, Luis Alejandro; Waksman De Torres, Noemí; Pérez-Meseguer, Jonathan; Torres-Lopez, Ernesto

    2018-01-15

    The plants examined in this study have previous biological activity reports indicating the possibility of found activity against herpes and cancer cell. The aim of this contribution was to carry out a screening of Juglans mollis (Juglandaceae), Persea americana (Lauraceae), Hamelia patens (Rubiaceae), Salvia texana (Lamiaceae), Salvia ballotaeflora (Lamiaceae), Ceanothus coeruleus (Rhamnaceae), Chrysactinia mexicana (Asteraceae) y Clematis drummondii (Ranunculaceae), against HeLa cells, VHS-1 and VHS-2. The method MTT was used to determine the 50% cytotoxic concentration (CC 50 ), in Vero and HeLa cell lines. To determine the 50% inhibitory concentration (IC 50 ) against herpes, the plaque reduction method was used. Results showed that none of the plants exhibited activity against HeLa cells. About antiherpetic activity, J. mollis and S. ballotaeflora extracts present antiherpetic activity in terms of their SI, increasingly interest for further studies on the isolation of compounds with antiherpetic activity and about the mechanisms of action that produce this activity.

  10. 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.

  11. Synthesis and chemiluminescent high throughput screening for inhibition of acetylcholinesterase activity by imidazo[2,1-b]thiazole derivatives.

    Science.gov (United States)

    Andreani, Aldo; Granaiola, Massimiliano; Guardigli, Massimo; Leoni, Alberto; Locatelli, Alessandra; Morigi, Rita; Rambaldi, Mirella; Roda, Aldo

    2005-12-01

    The synthesis of a new series of imidazo[2,1-b]thiazole derivatives is described. They were tested as acetylcholinesterase inhibitors by means of a chemiluminescent method suitable for high throughput screening. The compounds without quaternization had no appreciable inhibitory potency probably because they are poorly soluble in water. The corresponding quaternized compounds were good inhibitors with activity related to the spacer employed.

  12. 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...

  13. Stably transfected human cell lines as fluorescent screening assay for nuclear factor KB activation dependent gene expression

    Science.gov (United States)

    Hellweg, Christine E.; Baumstark-Khan, Christa; Horneck, Gerda

    2004-06-01

    Activation of the Nuclear Factor kappaB (NF-kappaB) pathway as a possible antiapoptotic route represents one important cellular stress response. For identifying conditions which are capable to modify this pathway, a screening assay for detection of NF-kappaB-dependent gene activation using the reporter proteins Enhanced Green Fluorescent Protein (EGFP) and its destabilized variant (d2EGFP) has been developed. Human Embryonic Kidney (HEK/293) cells were stably transfected with a vector carrying EGFP or d2EGFP under control of a synthetic promoter containing four copies of the NF-kappaB response element. Treatment with tumor necrosis factor alpha (TNF-alpha) gave rise to substantial EGFP / d2EGFP expression in up to 90 % of the cells and was therefore used to screen different stably transfected clones for induction of NF-kappaB dependent gene expression. The time course of d2EGFP expression after treatment with TNF-alpha or phorbol ester was measured using flow cytometry. Cellular response to TNF-alpha was faster than to phorbol ester. Treatment of cells with TNF-alpha and DMSO revealed antagonistic interactions of these substances in the activation NF-kappaB dependent gene expression. The detection of d2EGFP expression required FACS analysis or fluorescence microscopy, while EGFP could also be measured in the microplate reader, rendering the assay useful for high-throughput screening.

  14. Screening of Indonesian medicinal plants for inhibitor activity on nitric oxide production of RAW264.7 cells and antioxidant activity.

    Science.gov (United States)

    Choi, Eun-Mi; Hwang, Jae-Kwan

    2005-03-01

    Traditional Indonesian medicinal plants were screened for their inhibitory effects on the nitric oxide (NO) production in lipopolysaccharide (LPS)-stimulated RAW264.7 macrophages and for the antioxidant activity through the evaluation of free radical scavenging effect and reducing power. The results of screening indicated that 50 methanolic extracts inhibited (>50%) lipopolysaccharides (LPS)-induced NO release from RAW264.7 cells at 50 microg/ml, with 18 having greater than 100% inhibition. At 200 microg/ml, 61 methanol extracts exhibited inhibitory activity (>50%), with 45 showing greater than 100% inhibition. In addition, the free radical scavenging effects of 6 methanolic extracts were found to be more than 50% for extract concentration of 0.5 mug/ml. The results indicate that the extracts contain active compounds that inhibit NO release and scavenge free radical.

  15. Biological and analytical variations of 16 parameters related to coagulation screening tests and the activity of coagulation factors.

    Science.gov (United States)

    Chen, Qian; Shou, Weiling; Wu, Wei; Guo, Ye; Zhang, Yujuan; Huang, Chunmei; Cui, Wei

    2015-04-01

    To accurately estimate longitudinal changes in individuals, it is important to take into consideration the biological variability of the measurement. The few studies available on the biological variations of coagulation parameters are mostly outdated. We confirmed the published results using modern, fully automated methods. Furthermore, we added data for additional coagulation parameters. At 8:00 am, 12:00 pm, and 4:00 pm on days 1, 3, and 5, venous blood was collected from 31 healthy volunteers. A total of 16 parameters related to coagulation screening tests as well as the activity of coagulation factors were analyzed; these included prothrombin time, fibrinogen (Fbg), activated partial thromboplastin time, thrombin time, international normalized ratio, prothrombin time activity, activated partial thromboplastin time ratio, fibrin(-ogen) degradation products, as well as the activity of factor II, factor V, factor VII, factor VIII, factor IX, and factor X. All intraindividual coefficients of variation (CVI) values for the parameters of the screening tests (except Fbg) were less than 5%. Conversely, the CVI values for the activity of coagulation factors were all greater than 5%. In addition, we calculated the reference change value to determine whether a significant difference exists between two test results from the same individual. Thieme Medical Publishers 333 Seventh Avenue, New York, NY 10001, USA.

  16. 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.

  17. 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. Copyright © 2016 Elsevier Ltd. All rights reserved.

  18. Measurement of compliance with New York City's regulations on beverages, physical activity, and screen time in early child care centers.

    Science.gov (United States)

    Lessard, Laura; Lesesne, Catherine; Kakietek, Jakub; Breck, Andrew; Jernigan, Jan; Dunn, Lillian; Nonas, Cathy; O'Dell, Sarah Abood; Stephens, Robert L; Xu, Ye; Kettel Khan, Laura

    2014-10-16

    Policy interventions designed to change the nutrition environment and increase physical activity in child care centers are becoming more common, but an understanding of the implementation of these interventions is yet to be developed. The objective of this study was to explore the extent and consistency of compliance with a policy intervention designed to promote nutrition and physical activity among licensed child care centers in New York City. We used a multimethod cross-sectional approach and 2 independent components of data collection (Center Evaluation Component and Classroom Evaluation Component). The methods were designed to evaluate the impact of regulations on beverages served, physical activity, and screen time at child care centers. We calculated compliance scores for each evaluation component and each regulation and percentage agreement between compliance in the center and classroom components. Compliance with certain requirements of the beverage regulations was high and fairly consistent between components, whereas compliance with the physical activity regulation varied according to the data collection component. Compliance with the regulation on amount and content of screen time was high and consistent. Compliance with the physical activity regulation may be a more fluid, day-to-day issue, whereas compliance with the regulations on beverages and television viewing may be easier to control at the center level. Multiple indicators over multiple time points may provide a more complete picture of compliance - especially in the assessment of compliance with physical activity policies.

  19. 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, manufacturers, warehousing entities, distributors, third party logistics companies, and Indirect Air Carriers... supply chain to accept, screen, and transport air cargo. The uninterrupted collection of this information...

  20. Tuberculosis Screening and Active Tuberculosis among HIV-Infected Persons in a Canadian Tertiary Care Centre

    Directory of Open Access Journals (Sweden)

    Paul Brassard

    2009-01-01

    Full Text Available RATIONALE: HIV infection increases the risk of reactivation of latent tuberculosis (TB. The present study evaluates how latent TB is detected and treated to determine the effectiveness of screening in HIV-infected patients with diverse risk profiles.

  1. 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.

  2. Quercetin-loaded PLGA nanoparticles: a highly effective antibacterial agent in vitro and anti-infection application in vivo

    Science.gov (United States)

    Sun, Dongdong; Li, Nuan; Zhang, Weiwei; Yang, Endong; Mou, Zhipeng; Zhao, Zhiwei; Liu, Haiping; Wang, Weiyun

    2016-01-01

    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.

  3. Quercetin-loaded PLGA nanoparticles: a highly effective antibacterial agent in vitro and anti-infection application in vivo

    International Nuclear Information System (INIS)

    Sun, Dongdong; Li, Nuan; Zhang, Weiwei; Yang, Endong; Mou, Zhipeng; Zhao, Zhiwei; Liu, Haiping; Wang, Weiyun

    2016-01-01

    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

  4. [Enabling intervention for active screening of respiratory symptomatic patients in two municipalities located in the City of Havana province].

    Science.gov (United States)

    Jordán Severo, Tamine; Oramas González, René; Díaz Castrillo, Amparo Olga; Armas Pérez, Luisa; González Ochoa, Edilberto

    2010-01-01

    to evaluate the feasibility and immediate effect of an enabling intervention to improve the active screening of respiratory symptomatic patients in groups at risk of suffering tuberculosis and the quality of filling in lab records. a quasi-experimental-designed intervention study was conducted in two health areas of Boyeros municipality (Salvador Allende polyclinics and Federico Capdevila polyclinics). Two other areas were selected as controls in "10 de Octubre" municipality ("Turcios Lima" polyclinics and "Puente Uceda" polyclinics). Family physicians and nurses were then trained to identify patients with respiratory symptoms in the risk groups during home visits, finally sputum tests were indicated. A new model for lab recording was used. After 2 months, the ratio of detected respiratory symptomatic cases was estimated. The relative risk (95 % CI) was found. The percentage by type of screening, risk group and number of empty, misplaced and wrongly filled in items in the new model was calculated. after the intervention, the capabilities of physicians and nurses for detecting respiratory symptomatic patients in "Salvador Allende" health area was almost 2.5 times higher than before (RR= 2.4320) and in "Federico Capdevila" health area was almost 2 times higher (RR = 1.8112). Over 80 % of this improvement was due to active screening carried out almost completely (90 %) in risk groups. There were no misplaced or wrongly filled data, just empty items under 0.5%. the enabling intervention proved to be immediate and effective in order to raise the active screening of respiratory symptomatic patients in risk groups and to improve the quality of filling in lab records.

  5. A chemical screen in zebrafish embryonic cells establishes that Akt activation is required for neural crest development.

    Science.gov (United States)

    Ciarlo, Christie; Kaufman, Charles K; Kinikoglu, Beste; Michael, Jonathan; Yang, Song; D Amato, Christopher; Blokzijl-Franke, Sasja; den Hertog, Jeroen; Schlaeger, Thorsten M; Zhou, Yi; Liao, Eric; Zon, Leonard I

    2017-08-23

    The neural crest is a dynamic progenitor cell population that arises at the border of neural and non-neural ectoderm. The inductive roles of FGF, Wnt, and BMP at the neural plate border are well established, but the signals required for subsequent neural crest development remain poorly characterized. Here, we conducted a screen in primary zebrafish embryo cultures for chemicals that disrupt neural crest development, as read out by crestin:EGFP expression. We found that the natural product caffeic acid phenethyl ester (CAPE) disrupts neural crest gene expression, migration, and melanocytic differentiation by reducing Sox10 activity. CAPE inhibits FGF-stimulated PI3K/Akt signaling, and neural crest defects in CAPE-treated embryos are suppressed by constitutively active Akt1. Inhibition of Akt activity by constitutively active PTEN similarly decreases crestin expression and Sox10 activity. Our study has identified Akt as a novel intracellular pathway required for neural crest differentiation.

  6. 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.

  7. 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.

  8. piggyBac transposon somatic mutagenesis with an activated reporter and tracker (PB-SMART) for genetic screens in mice.

    Science.gov (United States)

    Landrette, Sean F; Cornett, Jonathan C; Ni, Thomas K; Bosenberg, Marcus W; Xu, Tian

    2011-01-01

    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.

  9. Anti-infectivity of camel polyclonal antibodies against hepatitis C virus in Huh7.5 hepatoma.

    Science.gov (United States)

    El-Fakharany, Esmail M; Abedelbaky, Nawal; Haroun, Bakry M; Sánchez, Lourdes; Redwan, Nezar A; Redwan, Elrashdy M

    2012-09-16

    To extend the study of the camel milk proteins which have antiviral activity against HCV, camel naïve polyclonal IgGs, α-lactalbumin were purified from camel milk and their anti-HCV effect was examined using PBMCs and Huh7.5 cell-lines. They were compared with the activity of human polyclonal IgGs and camel lactoferrin and casein. Three types of experiments were performed on PBMCs and HuH7.5 cell. HCV was directly incubated with the purified proteins and then mixed with both cell types, or the proteins were incubated with the cells and then exposed to HCV, or the HCV pre-infected cells were treated with the proteins to inhibit intracellular replication. The proteins were added to cells or virus at different concentrations and time intervals. Pretreated PBMCs and Huh7.5 cells with milk proteins were not protected when exposed to HCV infection. The direct interaction between HCV and camel IgGs and camel lactoferrin (cLf) led to a complete inhibition of HCV entry into cells, while casein, α-lactalbumin and human IgGs failed to inhibit HCV entry at any tested concentration. Camel IgGs showed ability to recognize HCV peptides with a significant titer (12 × 10(3)) in comparison with human IgGs which failed to do it. Camel lactoferrin was capable of inhibiting the intracellular HCV replication at concentrations of 0.25-1.25 mg/ml. Camel milk naïve polyclonal IgGs isolated from camel milk could inhibit the HCV infectivity and demonstrated strong signal against its synthetic peptides. Lactoferrin inhibit the HCV infectivity started from 0.25 mg/ml. However, α-lactalbumin, human IgGs and casein failed to demonstrate any activity against HCV infectivity.

  10. Anti-infectivity of camel polyclonal antibodies against hepatitis C virus in Huh7.5 hepatoma

    Directory of Open Access Journals (Sweden)

    EL-Fakharany Esmail M

    2012-09-01

    Full Text Available Abstract Purpose To extend the study of the camel milk proteins which have antiviral activity against HCV, camel naïve polyclonal IgGs, α-lactalbumin were purified from camel milk and their anti-HCV effect was examined using PBMCs and Huh7.5 cell-lines. They were compared with the activity of human polyclonal IgGs and camel lactoferrin and casein. Material and methods Three types of experiments were performed on PBMCs and HuH7.5 cell. HCV was directly incubated with the purified proteins and then mixed with both cell types, or the proteins were incubated with the cells and then exposed to HCV, or the HCV pre-infected cells were treated with the proteins to inhibit intracellular replication. The proteins were added to cells or virus at different concentrations and time intervals. Results Pretreated PBMCs and Huh7.5 cells with milk proteins were not protected when exposed to HCV infection. The direct interaction between HCV and camel IgGs and camel lactoferrin (cLf led to a complete inhibition of HCV entry into cells, while casein, α-lactalbumin and human IgGs failed to inhibit HCV entry at any tested concentration. Camel IgGs showed ability to recognize HCV peptides with a significant titer (12 × 103 in comparison with human IgGs which failed to do it. Camel lactoferrin was capable of inhibiting the intracellular HCV replication at concentrations of 0.25-1.25 mg/ml. Conclusion Camel milk naïve polyclonal IgGs isolated from camel milk could inhibit the HCV infectivity and demonstrated strong signal against its synthetic peptides. Lactoferrin inhibit the HCV infectivity started from 0.25 mg/ml. However, α-lactalbumin, human IgGs and casein failed to demonstrate any activity against HCV infectivity.

  11. Use of human immunoglobulins as an anti-infective treatment: the experience so far and their possible re-emerging role.

    Science.gov (United States)

    Bozzo, Jordi; Jorquera, Juan I

    2017-06-01

    Pooled human immunoglobulins (IGs) are prepared from plasma obtained from healthy donors as a concentrated antibody-containing solution. In addition, high-titer IGs (hyperimmune) against a specific pathogen can be obtained from vaccinated or convalescing donors. Currently, IGs can be used for the treatment of a variety of infections for which no specific therapy exists or that remain difficult to treat. Moreover, the recent pathogen outbreaks for which there is no approved treatment have renewed attention to the role of convalescent plasma and IGs. Areas covered: In this review, a historical perspective of the use of sera and IGs in humans as anti-infective agents (any viral, bacterial, parasitic infection), excluding immunodeficient patients, is presented from early development to the latest clinical studies. A Medline search was conducted to examine the peer-reviewed literature, with no date limits. Expert commentary: Human pooled plasma-derived IG products benefit from the polyclonal response of every individual donor and from the interindividual variability in such response. The trend to increased availability of vaccines for infectious diseases also opens new potential applications of hyperimmune IGs for emerging or re-emerging infectious diseases (e.g.: Ebola, Zika, Dengue), for the prevention and treatment in the general population, healthcare personnel and caregivers.

  12. 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 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.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.This study highlights the feasibility of obtaining novel alanine racemase inhibitor lead compounds by high-throughput screening for development of new anti-TB agents.

  13. In vitro evaluation of medicinal, antioxidant activities and phytochemical screening of iphiona grantioides and pluchea arguta subsp

    International Nuclear Information System (INIS)

    Naveed, S.; Ibrar, M.

    2016-01-01

    The crude ethanolic extracts (EE) derived from different parts of Iphiona grantioides (flower, leaf, stem and root) and Pluchea arguta subsp glabra Qaiser (leaf, stem and root) were screened In vitro for possible antioxidant, antibacterial, antifungal activities and phytochemical profile. Results for phytochemical screening revealed the presence of various important primary and secondary metabolites including carbohydrates, protein, essential oils, tannins, flavonoids, saponins, glycosides, phytosterol, tri-terphenoids and volatile oil in the ethanolic extracts (EE) of different parts of I. grantioides and P. arguta. Significant antibacterial activity was observed for flower and leaf (EE) of I. grantioides against Klebsiela pneumonia and Escherichia coli, while moderate antibacterial activity was showed by extracts from other parts of this plant. Similarly P. arguta leaf (EE) showed significant inhibitory activity against Escherichia coli, Pseudomonas aeroginosa and Micrococcus luteus than its stem and roots extract. The crude ethanolic extract of all parts of I. grantioides and P. arguta proved a rich source of fungicidal potential. Both the plants proved to have antioxidant potential by exhibiting DPPH radical scavenging activity. So it may be concluded from the present investigations that I. grantioides and P. arguta, both have a wide range of antibacterial, antifungal and antioxidant properties and can be utilized for the development of antimicrobial drugs for human beings, animals and as safe pesticides in agricultural practices as well as could be an important source of natural radical scavengers. (author)

  14. Depression Screening

    Science.gov (United States)

    ... Depression Screening Substance Abuse Screening Alcohol Use Screening Depression Screening (PHQ-9) - Instructions The following questions are ... this tool, there is also text-only version . Depression Screening - Manual Instructions The following questions are a ...

  15. Using constitutive activity to define appropriate high-throughput screening assays for orphan g protein-coupled receptors.

    Science.gov (United States)

    Ngo, Tony; Coleman, James L J; Smith, Nicola J

    2015-01-01

    Orphan G protein-coupled receptors represent an underexploited resource for drug discovery but pose a considerable challenge for assay development because their cognate G protein signaling pathways are often unknown. In this methodological chapter, we describe the use of constitutive activity, that is, the inherent ability of receptors to couple to their cognate G proteins in the absence of ligand, to inform the development of high-throughput screening assays for a particular orphan receptor. We specifically focus on a two-step process, whereby constitutive G protein coupling is first determined using yeast Gpa1/human G protein chimeras linked to growth and β-galactosidase generation. Coupling selectivity is then confirmed in mammalian cells expressing endogenous G proteins and driving accumulation of transcription factor-fused luciferase reporters specific to each of the classes of G protein. Based on these findings, high-throughput screening campaigns can be performed on the already miniaturized mammalian reporter system.

  16. The role of peer victimization in the physical activity and screen time of adolescents: a cross-sectional study.

    Science.gov (United States)

    Stearns, Jodie A; Carson, Valerie; Spence, John C; Faulkner, Guy; Leatherdale, Scott T

    2017-07-19

    Negative peer experiences may lead adolescents with overweight and obesity to be less active and engage in more sitting-related behaviors. Our study is among the first to empirically test these associations and hypothesized that 1) peer victimization would mediate the negative association between body weight status and moderate-to-vigorous physical activity (MVPA), and 2) peer victimization would mediate the positive association between body weight status and screen time. Differences by gender were also explored. Participants were a part of the Year 1 data (2012-2013) from the COMPASS study, a prospective cohort study of high school students in Ontario and Alberta, Canada. The final sample consisted of 18,147 students in grades 9 to 12 from 43 Ontario secondary schools. The predictor variable was weight status (non-overweight vs. overweight/obese), the mediator was peer victimization, and the outcome variables were screen time and MVPA. Multilevel path analysis was conducted, controlling for clustering within schools and covariates. A few differences were observed between males and females; therefore, the results are stratified by gender. For both males and females peer victimization partially mediated the association between weight status and screen time. Specifically, females with overweight/obesity reported 34 more minutes/day of screen time than did females who were not overweight and 2 of these minutes could be attributed to experiencing peer victimization. Similarly, males who were overweight/obese reported 13 more minutes/day of screen time than the males who were not overweight and 1 of these minutes could be attributed to experiencing more victimization. Males and females who were overweight/obese also reported less MVPA compared to those who were not overweight; however, peer victimization did not mediate these associations in the hypothesized direction. We found that higher rates of peer victimization experienced by adolescents with overweight and

  17. Phytochemical screening, antioxidant, anti-inflammatory and antiangiogenic activities of Lophira procera A. Chev. (Ochnaceae medicinal plant from Gabon

    Directory of Open Access Journals (Sweden)

    Rick-Leonid Ngoua-Meye-Misso

    2018-03-01

    Full Text Available The objective of this study was to perform phytochemical screening, to determine the content of phenolic compound, to evaluate antioxidant, anti-inflammatory and antiangiogenic activities of ethanol, water-ethanol and water extracts of Lophira procera. Antioxidant activity was determined by 2,2-diphenyl-1-picrylhydrazyl (DPPH and phosphomolybdenum assay, anti-inflammatory activity by proteins denaturation inhibition and membranes stabilization test and antiangiogenic activity by chicken chorioallantoic membrane (CAM method. The results showed that this plant is rich in saponins, polyphenols, tannins, total flavonoids, proanthocyanidins and coumarins. Extracts presented a strong antioxidant activity (IC50 values of 5.452 ± 0.119 μg/mL and 6.346 ± 0.544 μg/mL and respective AAI of 9.173 ± 0.203 and 7.919 ± 0.711. Excellent anti-inflammatory activity was also observed (IC50 = 16.952 ± 1.897 and IC50 = 23.172 ± 0.066 μg/mL for inhibition of protein denaturation and membrane stabilization respectively. Finally, extracts manifested a very good anti-angiogenic activity (with inhibitions ranging from 57.142 ± 0.124% to 100%. These biological activities are certainly due to high content of phenolic compound. This is the first study to report the phytochemical screening, the content of phenolic compound, the antioxidant, anti-inflammatory and antiangiogenic activities of extract derived from Lophira procera. The use of this plant in traditional medicine against ulcers, breast cancer, kidney and dental pain is therefore justified and its potential as a candidate for bioactive therapeutic molecule.

  18. 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

  19. N-Heterocyclic choline analogues based on 1,2,3,4-tetrahydro(iso)quinoline scaffold with anticancer and anti-infective dual action.

    Science.gov (United States)

    Zablotskaya, Alla; Segal, Izolda; Geronikaki, Athina; Shestakova, Irina; Nikolajeva, Vizma; Makarenkova, Galina

    2017-06-01

    Pharmacological effects of biologically active "small molecules" can be improved by their targeted modification, which affects drug delivery and interaction with tumor cells and microorganisms. We aimed to evaluate anticancer and antimicrobial activity of lipid-like choline derivatives modified via simultaneous introduction of tetrahydro(iso)quinoline based pharmacophore system at nitrogen atom and long chain alkyl substituent at oxygen atom. Target compounds were synthesized under phase-transfer catalysis conditions followed by quaternization, and evaluated for cytotoxicity and NO-generation ability on HT-1080 and MG-22A tumor cell lines and NIH 3T3 normal mouse fibroblasts, and screened for antimicrobial activity against gram-positive (Staphylococcus aureus and Bacillus cereus) and gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa and Proteus mirabilis) and fungi (Candida albicans and Aspergillus niger). Inhibitory action of active compounds towards E. coli DNA gyrase was investigated. Target compounds exhibit high selective cytotoxicity (LC 50 quinoline scaffold, possessing very high cytotoxicity with attendant strong antimicrobial activity are the leads for developing effective dual action therapeutics. Copyright © 2017 Institute of Pharmacology, Polish Academy of Sciences. Published by Elsevier Urban & Partner Sp. z o.o. All rights reserved.

  20. Virtual screening for selective allosteric mGluR1 antagonists and structure-activity relationship investigations for coumarine derivatives.

    Science.gov (United States)

    Noeske, Tobias; Jirgensons, Aigars; Starchenkovs, Igors; Renner, Steffen; Jaunzeme, Ieva; Trifanova, Dina; Hechenberger, Mirko; Bauer, Tanja; Kauss, Valerjans; Parsons, Christopher G; Schneider, Gisbert; Weil, Tanja

    2007-12-01

    A virtual screening study towards novel noncompetitive antagonists of the metabotropic glutamate receptor 1 (mGluR1) is described. Alignment-free topological pharmacophore descriptors (CATS) were used to encode the screening compounds. All virtual hits were characterized with respect to their allosteric antagonistic effect on mGluR1 in both functional and binding assays. Exceptionally high hit rates of up to 26 % were achieved, confirming the applicability of this virtual screening concept. Most of the compounds were found to be moderately active, however, one potent and subtype selective mGluR1 antagonist, 13 (IC(50): 0.362 microM, SEM +/-0.031; K(i): 0.753 microM, SEM +/-0.048), based on a coumarine scaffold was discovered. In a following activity optimization program a series of coumarine derivatives was synthesized. This led to the discovery of potent (60, IC(50): 0.058 microM, SEM +/-0.008; K(i): 0.293 microM, SEM +/-0.022) and subtype selective (rmGluR5 IC(50): 28.6 microM) mGluR1 antagonists. From our homology model of mGluR1 we derived a potential binding mode within the allosteric transmembrane region. Potential interacting patterns are proposed considering the difference of the binding pockets between rat and human receptors. The study demonstrates the applicability of ligand-based virtual screening for noncompetitive antagonists of a G-protein coupled receptor, resulting in novel, potent, and selective agents.

  1. In Silico Screening and In Vitro Activity Measurement of Javamide Analogues as Potential p38 MAPK Inhibitors.

    Science.gov (United States)

    Park, Jae B

    2017-12-13

    p38 Mitogen-activated protein kinase (p38 MAPK) is a protein kinase critically involved in the progress of inflammation/stress-associated diseases. Our data suggested that javamide analogues may contain strong anti-inflammation activities, but there is little information about their effects on p38 MAPK. Therefore, in this paper, the effects of thirty javamide analogues on p38 MAPK were investigated using in silico screening and in vitro p38 MAPK assay methods. The javamide analogues were synthesized and their chemical structures were confirmed using nuclear magnetic resonance (NMR) spectroscopic methods. Then, the javamide analogues were screened using an in silico modeling program. The screened analogues demonstrated a wide range of binding energy (ΔE; -20 to -39) and several analogues with ΔE; -34 to -39 showed strong binding affinity to p38 MAPK. In vitro p38 MAPK assay, the kinase was significantly inhibited by the analogues with great binding energy (ΔE; -34 to -39) and in silico scores (Avg. score; -27.5 to -29.3). Furthermore, the comparative analysis of both assays showed a positive correlation between the in silico scores and p38 MAPK inhibition. In fact, the javamide analogues with top five in silico scores (Avg. score; -27.5 to -29.3) were found to inhibit p38 MAPK by 27-31% ( p silico score (Avg. score; -29.2) inhibited p38 MAPK (IC 50 = 9.9 μM) a little better than its methyl ester with best in silico score (Avg. score; -29.3). To support the ability to inhibit p38 MAPK, the treatment of javamide-II-ethyl and -methyl esters could suppress the production of IL-8 and MCP-1 protein significantly by 22-73% ( p silico and in vitro assay approach may be a useful and efficient solution as a functional screening approach in searching new lead compounds for targeted molecules.

  2. Phytochemical Screening and Free-Radical Scavenging Activity of Bergenia stracheyi

    OpenAIRE

    Vinesh Kumar; Devendra Tyagi 2

    2013-01-01

    In an effort to reduce the undesirable consequences of synthetic food conservatives in human health and food industries, scientists have recently changed their interest to search new conservatives. Antioxidants are important inhibitors of lipid per-oxidation not only as a defense mechanism of living cells against oxidative damage but also for food preservation. The extracts prepared from Bergenia stracheyi herb were screened for flavonoids, tannins, alkaloids, saponins, terpenoids and glycosi...

  3. Fluorescence-based high-throughput screening of dicer cleavage activity

    Czech Academy of Sciences Publication Activity Database

    Podolská, Kateřina; Sedlák, David; Bartůněk, Petr; Svoboda, Petr

    2014-01-01

    Roč. 19, č. 3 (2014), s. 417-426 ISSN 1087-0571 R&D Projects: GA ČR GA13-29531S; GA MŠk(CZ) LC06077; GA MŠk LM2011022 Grant - others:EMBO(DE) 1483 Institutional support: RVO:68378050 Keywords : Dicer * siRNA * high-throughput screening Subject RIV: EB - Genetics ; Molecular Biology Impact factor: 2.423, year: 2014

  4. 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

  5. Phytochemical composition and in vitro screening of the antimicrobial activity of essential oils on oral pathogenic bacteria.

    Science.gov (United States)

    Tardugno, Roberta; Pellati, Federica; Iseppi, Ramona; Bondi, Moreno; Bruzzesi, Giacomo; Benvenuti, Stefania

    2018-03-01

    In this study, the activity of essential oils (EOs) against microorganisms involved in oral diseases was evaluated. Fourteen EOs were selected and subjected to gas chromatographic analysis, including Illicium verum, Eucaliptus globulus, Eugenia caryophyllata, Leptospermum scoparium, Mentha arvensis, Mentha piperita, Myrtus communis, Salvia officinalis, Melaleuca alternifolia, Rosmarinus officinalis, Lavandula x intermedia, Thymus capitatus and Thymus vulgaris. These EOs were tested for their antimicrobial activity on Streptococcus mutans and Lactobacillus species clinically isolated from dental surgery patients. The antibacterial activity was evaluated by means of the disc diffusion and the minimum inhibitory concentration (MIC). Five EOs, having shown an interesting antimicrobial activity, were selected for a second screening in combination between them and with chlorhexidine. From the second assays, two EO-EO and three EO-chlorhexidine associations gave interesting results as potential constituents of mouthwashes, especially for the contribution of oxygenated monoterpenes, including menthol, thymol and carvacrol.

  6. 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

    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...... 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......PAR(I-III) and suPAR(II-III) by 1-unit (ln-scale) was associated with a hazard ratio (HR) of 2.26 [95% confidence interval (CI) 1.17-4.35] and 2.53 (95% CI 1.56-4.10), respectively. There was a trend towards an increased risk of death from prostate cancer in screening-detected prostate cancer patients...

  7. [Evaluation of the anti-inflammatory activity and phytochemical screening of Annona senegalensis leaves].

    Science.gov (United States)

    Yeo, Dodehe; Dinica, Rodica; Yapi, Houphouet Felix; Furdui, Bianca; Praisler, Mirela; Djaman, Allico Joseph; N'Guessan, Jean David

    2011-01-01

    This study aims to highlight the anti-inflammatory activity of ethanol extract of Annona senegalensis and do its phytochemical screening. Rats were divided into three groups. The first group received only saline injection and instillation by intraperitoneal injection on days D0 and D7. This phase was the sensitization of that group. Then, on days D21, D22 and D23, the rats of the same group (Group 1) were injected with saline under anesthesia. The second group (Group 2) was composed of rats had not undergone treatment with the extract of Annona senegalensis. The rats in this batch have been sensitized by intraperitoneal injection (50 μL) of a solution of albumin (50 mg/rat) dissolved in aluminum hydroxide on days 0 and 7. Then during the challenge phase, saline containing 0.9% sodium chloride were injected intraperitoneally on days D21, D22 and D23. The sacrifice took place at D24 or 24 hours after the last challenge to ovalbumin. Similarly, rats of the third group (Group 3) have been sensitized by ovalbumin combined with aluminum hydroxide on days D0 and day D7. Then during the stage of provocation, rats in this batch received at days D21, D22 and D23, conjugated injection of albumin and ethanol extract of Annona senegalensis (injection of 0.4 mL of 7.10(-2) mg/kg body weight). The aqueous extract of Annona senegalensis has been previously prepared in saline. Twenty four hours after the last injection corresponding to D23, the rats were sacrificed under anesthesia. Secondary metabolites have been characterized by physico-chemical properties. Rats in the control (Group 1) gave an average of 24 ± 0.02 mast cells, 7 ± 0.1 macrophages, 9 ± 0.05 eosinophils. In the control group was not revealed the presence of neutrophils. Following the steps of provocation and awareness albumin (Group 2), we observed a significant increase in the number of inflammatory cells compared to control group (p Annona senegalensis (7.10(-2) mg/kg) induced a significant decrease in the

  8. THE UTILIZATION OF ACHATINA FULICA MUCUS IN ALGINATE MEMBRANE AS WOUND HEALING ACCELERATOR AND ANTI- INFECTION MATERIAL

    Directory of Open Access Journals (Sweden)

    Fatkhunisa Rahmawati

    2014-01-01

    Full Text Available Wound should be covered with bandage that is called wound dressing. Most people use synthetic materials such as gauze dressing. Gauze has high absorption of NaCl, which is often used to cleanse the wound. However, discomfort and pain arise since the gauze becomes sticky on the wound. Therefore, we need other alternatives instead of gauze to cover wound. One such alternative is the alginate membrane. This study used alginate membrane with mixture of mucous of the snail Achatina fulica, which contain proteins such as proline, serine asparagine, glycosaminoglycan, hydroxylysine, trionin and so forth, to activate the growth factor. Alginate powder and carboxymethl cellulose (CMC was dissolved in distilled water mixed with mucus of the snail Achatina fulica in four variations (4:0; 4:1, 4:2, 4:3 through a magnetic stirrer, and casted on a baking sheet covered with sterile gauze. High Performance Liquid Chromatography (HPLC test showed that the glycosaminoglycan content was found on the mucous of Achatina fulica. This was indicated by the appearance of peak at 325–350 second. The most optimum alginate and mucus composition was in ratio of 4:2. This ratio resulted in a wound dressing that was still able to absorb the exudate and optimally accelerated wound healing.

  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. Physical activity and screen time in children and adolescents in a medium size town in the South of Brazil.

    Science.gov (United States)

    Greca, João Paulo de Aguiar; Silva, Diego Augusto Santos; Loch, Mathias Roberto

    2016-09-01

    To analyze the associations between sex and age with behaviour related to physical activity practice and sedentary behaviour in children and adolescents. A cross-sectional study with 480 (236 boys) subjects enrolled in a public school in the city of Londrina, in the south of Brazil, aged 8-17 years. Measures of physical activity, sports practice and screen times were obtained using the Physical Activity Questionnaire for Older Children. The Mann-Whitney U test was used to compare variables between boys and girls. The Chi squared test was used for categorical analysis and Poisson regression was used to identify prevalence. Girls (69.6%; PR=1.05 [0.99-1.12]) spent more time with sedentary behaviour than boys (62.2%). Boys (80%; PR=0.95 [0.92-0.98]) were more physically active than girls (91%). Older students aged 13-17 showed a higher prevalence of physical inactivity (91.4%; PR=1.06 [1.02-1.10]) and time spent with sedentary behaviour of ≥2h/day (71.8%; PR=0.91 [0.85-0.97]) when compared to younger peers aged 8-12 (78.7 and 58.5%, respectively). The prevalence of physical inactivity was higher in girls. Older students spent more screen time in comparison to younger students. Copyright © 2016 Sociedade de Pediatria de São Paulo. Publicado por Elsevier Editora Ltda. All rights reserved.

  11. A screening method for cytochrome P-450 organic peroxidase activity and application to hydrocarbon-degrading bacterial populations

    Energy Technology Data Exchange (ETDEWEB)

    Wyndham, R.C. (Univ. of Toronto, ON (Canada))

    1987-01-01

    A method to detect the expression of hemoproteins with organic hydroperoxide reducing activity was developed to screen bacterial populations isolated from heavy oils and oil sands. The method is based on the activity of cytochrome P-450 as catalyst in the reduction of cumene hydroperoxide by artificial electron donors. There was no cross-reactivity with true catalyst in the reduction of cumene hydroperoxide by artificial electron donors. There was no cross-reactivity with true peroxidases involved in the reduction of hydrogen peroxide. Cross-reactivity with catalase could be eliminated with appropriate inhibitors but did not normally interfere with the detection method. A preliminary screen resulted in the isolation of Acinetobactor calcoaceticus and a range of Gram-positive bacteria with organic peroxidase activity. Carbon monoxide difference spectra of cell-free extracts of the isolates revealed the presence of a hydrocarbon-inducible cytochrome P-450 in Acinetobacter calcoaceticus and in coryneform and actinomycete bacteria. A CO-binding cytochrome of unknown type with a Soret absorption maximum at 424 nm and cumene hydroperoxidase activity was also detected in some strains. 34 refs., 1 fig., 3 tabs.

  12. High-Throughput Screening of a Collection of Known Pharmacologically Active Small Compounds for Identification of Candida albicans Biofilm Inhibitors

    Science.gov (United States)

    Siles, Samuel A.; Srinivasan, Anand; Pierce, Christopher G.

    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 Library, to identify inhibitors of C. albicans biofilm formation. According to their pharmacological applications that are currently known, we classified these bioactive compounds as antifungal drugs, as antimicrobials/antiseptics, or as miscellaneous drugs, which we considered to be drugs with no previously characterized antifungal activity. Using a 96-well microtiter plate-based high-content screening assay, we identified 38 pharmacologically active agents that inhibit C. albicans biofilm formation. These drugs were subsequently tested for their potency and efficacy against preformed biofilms, and we identified three drugs with novel antifungal activity. Thus, repurposing FDA-approved drugs opens up a valuable new avenue for identification and potentially rapid development of antifungal agents, which are urgently needed. PMID:23689719

  13. Using information from historical high-throughput screens to predict active compounds.

    Science.gov (United States)

    Riniker, Sereina; Wang, Yuan; Jenkins, Jeremy L; Landrum, Gregory A

    2014-07-28

    Modern high-throughput screening (HTS) is a well-established approach for hit finding in drug discovery that is routinely employed in the pharmaceutical industry to screen more than a million compounds within a few weeks. However, as the industry shifts to more disease-relevant but more complex phenotypic screens, the focus has moved to piloting smaller but smarter chemically/biologically diverse subsets followed by an expansion around hit compounds. One standard method for doing this is to train a machine-learning (ML) model with the chemical fingerprints of the tested subset of molecules and then select the next compounds based on the predictions of this model. An alternative approach would be to take advantage of the wealth of bioactivity information contained in older (full-deck) screens using so-called HTS fingerprints, where each element of the fingerprint corresponds to the outcome of a particular assay, as input to machine-learning algorithms. We constructed HTS fingerprints using two collections of data: 93 in-house assays and 95 publicly available assays from PubChem. For each source, an additional set of 51 and 46 assays, respectively, was collected for testing. Three different ML methods, random forest (RF), logistic regression (LR), and naïve Bayes (NB), were investigated for both the HTS fingerprint and a chemical fingerprint, Morgan2. RF was found to be best suited for learning from HTS fingerprints yielding area under the receiver operating characteristic curve (AUC) values >0.8 for 78% of the internal assays and enrichment factors at 5% (EF(5%)) >10 for 55% of the assays. The RF(HTS-fp) generally outperformed the LR trained with Morgan2, which was the best ML method for the chemical fingerprint, for the majority of assays. In addition, HTS fingerprints were found to retrieve more diverse chemotypes. Combining the two models through heterogeneous classifier fusion led to a similar or better performance than the best individual model for all assays

  14. 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...

  15. Recruitment, screening, and baseline participant characteristics in the WALK 2.0 study: A randomized controlled trial using web 2.0 applications to promote physical activity

    Directory of Open Access Journals (Sweden)

    Cristina M. Caperchione

    2016-04-01

    Conclusion: The results of this recruitment process demonstrate the successful use of multiple strategies to obtain a diverse sample of adults eligible to take part in a web-based physical activity promotion intervention. The use of dual screening processes ensured safe participation in the intervention. This approach to recruitment and physical activity screening can be used as a model for further trials in this area.

  16. New agents with potential leishmanicidal activity identified by virtual screening of chemical databases: New agents with potential leishmanicidal activity

    Directory of Open Access Journals (Sweden)

    Juan Rebollo

    2013-04-01

    Full Text Available Introduction and Objectives: Leishmaniosis, a disease caused by a protozoan parasite, remains a serious public health problem threatening about 350 million people around the world, of which 12 million are believed to be currently infected (WHO 2010. To date, there are no vaccines against the species of parasites and the treatment is based only on chemotherapy with toxic-, expensive- and inefficient- drugs. There is an urgent need for better drugs against Leishmania, the etiological agent of the disease. The main anti-leishmanial drug used in Colombia is meglumineantimoniate [chemical name according to the International Union of Pure and Applied Chemistry (IUPAC: Hydroxy-dioxostiborane; (2R,3R,4R,5S- 6-methylaminohexane-1,2,3,4,5-pentol, (C7H17NO5], which is not efficient in the treatment of infections caused by Leishmania braziliensis, the most prevalent specie in the Caribbean coast of Colombia. Methods: We performed an in silico virtual screening of several datasets including ChemBridge and Pubchem. We virtually screened a total of 28.755 compounds against a 3D model of 6-phosphoglucono -lactonase (6-PGL from Leishmania braziliensis to identify novel inhibitors.Molecular docking of databases was performed using the software Sybyl 8.0 and AutoDockVina. Results: The initial virtual screening using a structure-based method identified 10 compounds, which were later tested with AutodockVina and classified according to their docking scores. Conclusions: These novel and potential inhibitors constitute new drug candidates that must be biologically tested to define their value as an alternative chemotherapeutic agent in the treatment of these protozoan infections. Salud UIS 2013; 45 (1: 33-40

  17. In vitro thrombolytic, anthelmintic, anti-oxidant and cytotoxic activity with phytochemical screening of methanolic extract of Xanthium indicum leaves

    Directory of Open Access Journals (Sweden)

    Antara Ghosh

    2015-12-01

    Full Text Available Xanthium indicum is an important medicinal plant traditionally used in Bangladesh as a folkloric treatment. The current study was undertaken to evaluate thrombolytic, anthelmintic, anti-oxidant, cytotoxic properties with phytochemical screening of methanolic extract of X. indicum leaves. The analysis of phytochemical screening confirmed the existence of phytosetrols and diterpenes. In thrombolytic assay, a significant clot lysis was observed at four concentrations of plant extract compare to the positive control streptokinase (30,000 IU, 15,000 IU and negative control normal saline. The extract revealed potent anthelmintic activity at different concentrations. In anti-oxidant activity evaluation by two potential experiments namely total phenolic content determination and free radical scavenging assay by 2, 2-diphenylpicrylhydrazyl (DPPH, the leaves extract possess good anti-oxidant property. In the brine shrimp lethality bioassay, the crude extract showed potent (LC50 1.3 μg/mL cytotoxic activity compare to the vincristine sulfate as a positive control (LC50 0.8 μg/mL.

  18. 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

  19. Demographic correlates of screen time and objectively measured sedentary time and physical activity among toddlers: a cross-sectional study

    Directory of Open Access Journals (Sweden)

    Valerie Carson

    2017-02-01

    Full Text Available Abstract Background Determining the most important demographic correlates of sedentary behavior and physical activity will help identify the groups of children that are most in need of intervention. Little is known in regards to the demographic correlates of sedentary behavior and physical activity in toddlers (aged 12–35 months, where long-term behavioral patterns may initially be formed. Therefore, the objective of this study was to examine the associations between demographic correlates and specific types of sedentary behavior and physical activity in this age group. Methods Findings are based on 149 toddlers (19.0 ± 1.9 months and their parents (33.7 ± 4.7 years recruited from immunization clinics in Edmonton, Canada as part of the Parents’ Role in Establishing healthy Physical activity and Sedentary behavior habits (PREPS project. Toddlers’ and parental demographic characteristics and toddlers’ television viewing, video/computer games, and overall screen time were measured via the PREPS parental questionnaire. Toddlers’ objectively measured sedentary time and physical activity (light, moderate to vigorous, and total were accelerometer-derived using Actigraph wGT3X-BT monitors. Simple and multiple linear regression models were conducted to examine associations. Results In the multiple linear regression models, toddlers’ age, toddlers’ sex (female versus male, toddlers’ race/ethnicity (other versus European-Canadian/Caucasian, and household income ($50,001 to $100,000 versus > $100,000 were significantly positively associated, and main type of child care (child care center versus parental care was significantly negatively associated with screen time. Similar findings were observed with television viewing, except null associations were observed for toddlers’ sex. Toddlers’ race/ethnicity (other versus European-Canadian/Caucasian was significantly positively associated and main type of child care (child care

  20. Demographic correlates of screen time and objectively measured sedentary time and physical activity among toddlers: a cross-sectional study.

    Science.gov (United States)

    Carson, Valerie; Kuzik, Nicholas

    2017-02-13

    Determining the most important demographic correlates of sedentary behavior and physical activity will help identify the groups of children that are most in need of intervention. Little is known in regards to the demographic correlates of sedentary behavior and physical activity in toddlers (aged 12-35 months), where long-term behavioral patterns may initially be formed. Therefore, the objective of this study was to examine the associations between demographic correlates and specific types of sedentary behavior and physical activity in this age group. Findings are based on 149 toddlers (19.0 ± 1.9 months) and their parents (33.7 ± 4.7 years) recruited from immunization clinics in Edmonton, Canada as part of the Parents' Role in Establishing healthy Physical activity and Sedentary behavior habits (PREPS) project. Toddlers' and parental demographic characteristics and toddlers' television viewing, video/computer games, and overall screen time were measured via the PREPS parental questionnaire. Toddlers' objectively measured sedentary time and physical activity (light, moderate to vigorous, and total) were accelerometer-derived using Actigraph wGT3X-BT monitors. Simple and multiple linear regression models were conducted to examine associations. In the multiple linear regression models, toddlers' age, toddlers' sex (female versus male), toddlers' race/ethnicity (other versus European-Canadian/Caucasian), and household income ($50,001 to $100,000 versus > $100,000) were significantly positively associated, and main type of child care (child care center versus parental care) was significantly negatively associated with screen time. Similar findings were observed with television viewing, except null associations were observed for toddlers' sex. Toddlers' race/ethnicity (other versus European-Canadian/Caucasian) was significantly positively associated and main type of child care (child care center, day home, other versus parental care) was significantly

  1. 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.

  2. 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.

  3. Intra-specific differentiation of fungal endosymbiont Alternaria longissima CLB44 using RNA secondary structure analysis and their anti-infective potential.

    Science.gov (United States)

    Rao, H C Yashavantha; Satish, Sreedharamurthy

    2016-08-01

    New antimicrobial agents derived from endosymbio-tic fungi with unique and targeted mode of action are crucially rudimentary to combat multidrug-resistant infections. Most of the fungi isolated as endosymbionts show close morphological feature resemblance to plant pathogenic or free-living forms, and it is difficult to differentiate these different lifestyles. A fungal endosymbiont strain CLB44 was isolated from Combretum latifolium Blume (Combretaceae). CLB44 was then identified as Alternaria longissima based on morphological and internal transcribed spacer (ITS) intervening 5.8S rRNA gene sequence analysis. ITS2 RNA secondary structure analysis was carried out using mfold server with temperature 37 °C, and anti-infective potential was determined by MIC and disk diffusion methods. ITS2 RNA secondary structure analysis clearly distinguished endosymbiotic A. longissima CLB44 from free-living and pathogenic A. longissima members in the same monophyletic clade. Secondary metabolites produced effectively inhibited Pseudomonas aeruginosa (25 μg/ml), Escherichia coli (25 μg/ml), methicillin-resistant Staphylococcus aureus (50 μg/ml), Candida albicans (100 μg/ml), and other human pathogens. This study emerges as an innovative finding that explores newly revealed ITS2 RNAs that may be an insight as new markers for refining phylogenetic relations and to distinguish fungal endosymbionts with other free-living or pathogenic forms. A. longissima CLB44, in the emerging field of endosymbionts, will pave the way to a novel avenue in drug discovery to combat multidrug-resistant infections. The sequence data of this fungus is deposited in GenBank under the accession no. KU310611.

  4. A high throughput amenable Arabidopsis-P. aeruginosa system reveals a rewired regulatory module and the utility to identify potent anti-infectives.

    Directory of Open Access Journals (Sweden)

    Suresh Gopalan

    2011-01-01

    Full Text Available We previously demonstrated that in a metasystem consisting of Arabidopsis seedlings growing in liquid medium (in 96 well plates even microbes considered to be innocuous such as laboratory strains of E. coli and B. subtilis can cause potent damage to the host. We further posited that such environment-induced adaptations are brought about by 'system status changes' (rewiring of pre-existing cellular signaling networks and components of the host and the microbe, and that prolongation of such a situation could lead to the emergence of pathogenic states in real-life. Here, using this infection model, we show that the master regulator GacA of the human opportunistic pathogen P. aeruginosa (strain PA14 is dispensable for pathogenesis, as evidenced by three independent read-outs. The gene expression profile of the host after infection with wild type PA14 or the gacA mutant are also identical. GacA normally acts upstream of the quorum sensing regulatory circuit (that includes the regulator LasR that controls a subset of virulence factors. Double mutants in gacA and lasR behave similar to the lasR mutant, as seen by abrogation of a characteristic cell type specific host cell damage caused by PA14 or the gacA mutant. This indicates that a previously unrecognized regulatory mechanism is operative under these conditions upstream of LasR. In addition, the detrimental effect of PA14 on Arabidopsis seedlings is resistant to high concentrations of the aminoglycoside antibiotic gentamicin. These data suggest that the Arabidopsis seedling infection system could be used to identify anti-infectives with potentially novel modes of action.

  5. A high throughput amenable Arabidopsis-P. aeruginosa system reveals a rewired regulatory module and the utility to identify potent anti-infectives.

    Science.gov (United States)

    Gopalan, Suresh; Ausubel, Frederick M

    2011-01-21

    We previously demonstrated that in a metasystem consisting of Arabidopsis seedlings growing in liquid medium (in 96 well plates) even microbes considered to be innocuous such as laboratory strains of E. coli and B. subtilis can cause potent damage to the host. We further posited that such environment-induced adaptations are brought about by 'system status changes' (rewiring of pre-existing cellular signaling networks and components) of the host and the microbe, and that prolongation of such a situation could lead to the emergence of pathogenic states in real-life. Here, using this infection model, we show that the master regulator GacA of the human opportunistic pathogen P. aeruginosa (strain PA14) is dispensable for pathogenesis, as evidenced by three independent read-outs. The gene expression profile of the host after infection with wild type PA14 or the gacA mutant are also identical. GacA normally acts upstream of the quorum sensing regulatory circuit (that includes the regulator LasR) that controls a subset of virulence factors. Double mutants in gacA and lasR behave similar to the lasR mutant, as seen by abrogation of a characteristic cell type specific host cell damage caused by PA14 or the gacA mutant. This indicates that a previously unrecognized regulatory mechanism is operative under these conditions upstream of LasR. In addition, the detrimental effect of PA14 on Arabidopsis seedlings is resistant to high concentrations of the aminoglycoside antibiotic gentamicin. These data suggest that the Arabidopsis seedling infection system could be used to identify anti-infectives with potentially novel modes of action.

  6. 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.

  7. Screening for improved activity of a transglutaminase from Streptomyces mobaraensis created by a novel rational mutagenesis and random mutagenesis.

    Science.gov (United States)

    Yokoyama, Keiichi; Utsumi, Hiroe; Nakamura, Takefumi; Ogaya, Daisuke; Shimba, Nobuhisa; Suzuki, Eiichiro; Taguchi, Seiichi

    2010-08-01

    Microbial transglutaminase (MTG) has been used extensively in academic research and the food industries through its cross-linking or posttranslational modification of proteins. Two enzyme engineering approaches were applied to improve MTG activity. One is a novel method of rational mutagenesis, called water-accessible surface hot-space region-oriented mutagenesis (WASH-ROM). One hundred and fifty-one point mutations were selected at 40 residues, bearing high solvent-accessibility surface area, within a 15 A space from the active site Cys64. Among them, 32 mutants showed higher specific activity than the wild type. The other is a random mutagenesis of the whole region of the MTG gene, coupled with a new plate assay screening system, using Corynebacterium Expression System CORYNEX. This in vivo system allowed us to readily distinguish the change in enzymatic activity by monitoring the intensity of enzymatic reaction-derived color zones surrounding recombinant cells. From the library of 24,000 mutants, ten were finally selected as beneficial mutants exhibiting higher specific activity than the wild type. Furthermore, we found that Ser199Ala mutant with additional N-terminal tetrapeptide showed the highest specific activity (1.7 times higher than the wild type). These various beneficial positions leading to increased specific activity of MTG were identified to achieve further enzyme improvements.

  8. 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.

  9. 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

    than 50 mu M. The positive control 4-hydroxyandrostendione (1 mu M) 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...

  10. 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...

  11. Use of Quantitative Structure-Activity Relationship (QSAR) and ADMET prediction studies as screening methods for design of benzyl urea derivatives for anti-cancer activity.

    Science.gov (United States)

    Lokwani, Deepak; Bhandari, Shashikant; Pujari, Radha; Shastri, Padma; Shelke, Ganesh; Pawar, Vidya

    2011-06-01

    2D and 3D quantitative structure-activity relationship studies have been carried out for establishing a correlation between the structural properties of benzyl urea derivatives and their anti-tumour activities. From this correlation, the new chemical entities were designed, and their activity and absorption, distribution, metabolism, excretion, and toxicity properties were also predicted. Finally, the most promising compounds from these screening were synthesized and biologically evaluated for their anti-cancer properties. Compound 1-(2, 4-dimethylphenyl)-3, 3-dimethyl-1-(2-nitrobenzyl) urea (7d) showed significant anti-proliferative activity (at 100 µg/mL) in human cancer cell lines-T-cell leukemia (Jurkat J6), myelogenous leukemia (K562), and breast cancer (MCF-7) compared to reference standard 5-flurouracil.

  12. Risk of active tuberculosis in patients with inflammatory arthritis receiving TNF inhibitors: a look beyond the baseline tuberculosis screening protocol.

    Science.gov (United States)

    Soare, Alina; Gheorghiu, Ana Maria; Aramă, Victoria; Bumbăcea, Dragoș; Dobrotă, Rucsandra; Oneaţă, Raida; Pintilie, Simona; Milicescu, Mihaela; Ancuţa, Ioan; Martin, Andrei; Sasu, Mariana; Ciofu, Claudia; Macovei, Liviu; Stoica, Victor; Bojincă, Mihai; Mihai, Carina

    2017-11-17

    Tuberculosis (TB) is a major concern in patients receiving TNF inhibitors (TNFi). This study aimed to assess the incidence of active TB and the efficacy of TB prevention measures used over the years, and to determine risk factors for developing TB, in a single-centre cohort of patients with rheumatoid arthritis (RA), psoriatic arthritis (PsA) and ankylosing spondylitis (AS) receiving TNFi. Data of all patients in whom treatment with TNFi was initiated in our rheumatology clinic until December 1st 2014 have been retrospectively analysed. The cohort was divided into 3 groups per the mandatory LTBI screening method at baseline: tuberculin skin test (TST) with a positive threshold of either 10 mm (group TST1), or 5 mm (group TST2), and QuantiFERON®-TB Gold test (group QFT). The incidence of active TB was analysed for each group and compared to TB incidence data in general population. Five hundred fifty patients were included (305 RA, 42 PsA, 203 AS); 97 patients belonged to the TST1, 229 to the TST2 and 224 to the QFT group. The number of active TB cases/time of exposure to TNFi (person-years, PY) was 8/593.5, 9/1044.0 and 3/555.3, respectively, accounting for an incidence of 1348.0, 862.1 and 540.2 cases per 10 5 PY. Active TB cases occurring in the first year of TNFi treatment (early TB) per total TB cases were only 3/8, 1/9 and 1/3, respectively, too few to identify statistically significant differences between the 3 LTBI screening protocols. However, less TB cases per total observation time were registered in the QFT group, probably due to the reduced duration of exposure to TNFi. All cases of active TB were registered among patients receiving monoclonal antibodies TNFi agents. We have found no significant risk factors for developing active TB. In our cohort, TB occurring after 1 year of TNFi treatment exceeds 'early TB', suggesting the necessity of further TB prevention measures besides baseline screening for LTBI.

  13. 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

  14. A multi-assay screening approach for assessment of endocrine-active contaminants in wastewater effluent samples

    International Nuclear Information System (INIS)

    Metcalfe, Chris D.; Kleywegt, Sonya; Letcher, Robert J.; Topp, Edward; Wagh, Purva; Trudeau, Vance L.; Moon, Thomas W.

    2013-01-01

    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

  15. Screening for antibacterial and antibiofilm activity in Thai medicinal plant extracts against oral microorganisms

    OpenAIRE

    Teanpaisan, Rawee; Kawsud, Pajaree; Pahumunto, Nuntiya; Puripattanavong, Jindaporn

    2016-01-01

    To evaluate the antibacterial activity of 12 ethanol extracts of Thai traditional herb against oral pathogens. The antibacterial activities were assessed by agar well diffusion, broth microdilution, and time-kill methods. Antibiofilm activity was investigated using a 3-[4,5-dimethyl-2-thiazolyl]-2,5-diphenyl-2H-tetrazolium-bromide (MTT) assay. High performance liquid chromatography (HPLC), thin layer chromatography (TLC) fingerprinting, and TLC-bioautography were used to determine the active ...

  16. High-throughput screen identifies small molecule inhibitors targeting acetyltransferase activity of Mycobacterium tuberculosis GlmU.

    Science.gov (United States)

    Rani, Chitra; Mehra, Rukmankesh; Sharma, Rashmi; Chib, Reena; Wazir, Priya; Nargotra, Amit; Khan, Inshad Ali

    2015-12-01

    N-acetylglucosamine-1-phosphate uridyltransferase (GlmU) is a pivotal bifunctional enzyme, its N and C terminal domains catalyzes uridyltransferase and acetyltransferase activities, respectively. Final product of GlmU catalyzed reaction, uridine-diphospho-N-acetylglucosamine (UDP-GlcNAc), acts as sugar donor providing GlcNAc residues in the synthesis of peptidoglycan and a disaccharide linker (D-N-GlcNAc-1-rhamnose), the key structural components of Mycobacterium tuberculosis (M. tuberculosis) cell wall. In the present study, we have searched new inhibitors against acetyltransferase activity of M. tuberculosis GlmU. A subset of 1607 synthetic compounds, selected through dual approach i.e., in-silico and whole cell screen against 20,000 compounds from ChemBridge library, was further screened using an in-vitro high throughput bioassay to identify inhibitors of acetyltransferase domain of M. tuberculosis GlmU. Four compounds were found to inhibit GlmU enzyme specific to acetyltransferase activity, with IC50 values ranging from 9 to 70 μM. Two compounds (6624116, 5655606) also exhibited whole cell activity against drug susceptible as well as drug resistant M. tuberculosis. These two compounds also exhibited increased anti-TB activity when tested in combination with rifampicin, isoniazid and ethambutol, however 5655606 was cytotoxic to eukaryotic cell line. These results demonstrate that identified chemical scaffolds can be used as inhibitors of M. tuberculosis cell wall enzyme after optimizations for future anti-TB drug development program. Copyright © 2015 Elsevier Ltd. All rights reserved.

  17. [Screening of anti-inflammatory and analgesic activities in marines macroalgae from Mediterranean Sea].

    Science.gov (United States)

    Chatter Riahi, R; Tarhouni, S; Kharrat, R

    2011-01-01

    Methanolic extracts of 13 seaweeds collected from the Mediterranean sea (Tunisian, Moroccan and Greek coasts) from different classes (Chlorophycae, Pheopbycae and Rhodophycae) are testedfor their analgesic and antiinflammatory effects. These activities were estimated in vivo, respectively by writhing test and carrageenan test. Nine species among 13 tested seaweeds showed an important analgesic activity. On the other hand only 5 seaweeds showed a significant anti-inflammatory activity (Cystoseira barbata and Sargassum vulgare) had endowed with the double analgesic and anti-inflammatory activity. The red algae Geliduim sesquipedale have only anti-inflammatory activity and the other one endowed only with an analgesic activity (Enteromorpha compressa, Chaetomorpha linum, Cystoseira ericoidies, Sacchoriza bulbosa et Corralina officinalis). The simultaneous or individual presence of the analgesic and\\or anti-inflammatory activities of the various extracts can find its application in the therapeutic domain.

  18. 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.

  19. Insecticidal activity of three plants extracts against Myzus persicae (Sulzer, 1776 and their phytochemical screening

    Directory of Open Access Journals (Sweden)

    Billal NIA

    2015-11-01

    Full Text Available To reduce the use of synthetic pesticides and their negative effects on the environment, leaves extracts of Artemisia herba-alba Asso, Eucalyptus camaldulensis Dehnh and Rosmarinus officinalis L. were obtained with petroleum ether, ethanol and distilled water as solvents. These extracts were evaluated under laboratory conditions for their insecticidal effect against 3 to 4 days-old Myzus persicae individuals (Homoptera: Aphididae at 1, 2.5, 5, and 10 %. We made observations after 24 hours. Etheric extract of all plants was effective and caused mortalities (100 %, 53 % and 60 % respectively at the highest concentration. However, ethanolic and aqueous extracts did not show any significant insecticidal effect. The phytochemical screening showed the richness of etheric extract in terpenes. The results obtained suggest that we can make bioinsecticides based on leaves etheric extracts from these plants for use in integrated pest management.

  20. Screening of marine fungus from Nanji Island and activity of their metabolites against pathogenic Vibrio from Pseudosciaena crocea

    Science.gov (United States)

    Zhao, Shujiang; Li, Shuping; Liu, Huihui; Zhao, Qian; Wang, Jieyou; Yan, Maocang

    2012-09-01

    Seventy-eight marine fungal strains were isolated from sediment samples collected off the coast of Nanji Island, Wenzhou, Zhejiang Province, China. Antibacterial screening using the agar disc method showed that 19 of the isolated strains could inhibit at least one pathogenic V ibrio from P seudosciaena crocea. Subsequent screening confirmed that nine strains produced antibacterial metabolites that had activity against one or several types of pathogenic V ibrio. Strain NJ0104 had the widest antimicrobial spectrum and strong activity, particularly against Vibrio parahaemolyticus-MM0810072. A preliminary study of NJ0104 antibacterial metabolites demonstrated that they had thermal stability up to 80°C, ultraviolet stability up to 40 min and pH stability between 4.0-7.0. In addition, the antibacterial metabolites were readily soluble in butanol. To identify the specific strain, the ITS-5.8S rDNA regions of NJ0104 were PCR amplified and sequenced. Based on the combination of phenotypic and genotypic data, the strain was identified as Arthrinium sp.

  1. Newborn Screening

    Science.gov (United States)

    ... Laboratory Sciences Office of Public Health Genomics Publications & Articles Newborn Screening Lab Bulletin Laboratory Partners Multimedia Tools Newborn Screening Program – Role of Laboratories Meet the Scientist Newborn Screening: Family Stories Newborn Screening: Public Health ...

  2. Multidimensional Screening with Complementary Activities: Regulating a Monopolist with Unknown Cost and Unknown Preference for Empire Building

    Directory of Open Access Journals (Sweden)

    Didier Laussel

    2013-09-01

    Full Text Available We study the optimal regulation of a monopolist when intrinsic efficiency (intrinsic cost and empire building tendency (marginal utility of output are private information, but actual cost (the difference between intrinsic cost and effort level is observable. This is a problem of multidimensional screening with complementary activities. Results are not only driven by the prior probabilities of the four possible types, but also by the relative magnitude of the uncertainty along the two dimensions of private information. If the marginal utility of output varies much more (less across managers than the intrinsic marginal cost, there is empire building (efficiency dominance. In that case, an inefficient empire builder produces more (less and at lower (higher marginal cost than an efficient money-seeker. It is only when variabilities are similar that there may be the natural ranking of activities (empire builders produce more, while efficient managers produce at a lower cost.

  3. Screening extracts of Achyranthes japonica and Rumex crispus for activity against various plant pathogenic fungi and control of powdery mildew.

    Science.gov (United States)

    Kim, Jin-Cheol; Choi, Gyung Ja; Lee, Seon-Woo; Kim, Jin-Seog; Chung, Kyu Young; Cho, Kwang Yun

    2004-08-01

    Methanol extracts of fresh materials of 183 plants were screened for in vivo antifungal activity against Magnaporthe grisea, Corticium sasaki, Botrytis cinerea, Phytophthora infestans, Puccinia recondita and Erysiphe graminis f sp hordei. Among them, 33 plant extracts showed disease-control efficacy of more than 90% against at least one of six plant diseases. The methanol extracts of Achyranthes japonica (whole plant) and Rumex crispus (roots) at concentrations greater than 11 g fresh weight of plant tissue per litre of aqueous Tween 20 solution effectively controlled the development of barley powdery mildew caused by E graminis f sp hordei in an in vivo assay using plant seedlings. At a concentration of 300 g fresh weight of plant tissue per litre of Tween 20 solution, the two extracts were as efficient as the fungicide fenarimol (30 mg litre(-1)) and more active than the fungicide polyoxin B (100 and 33 mg litre(-1)) against Sphaerotheca fuliginea on cucumber plants in glasshouse trials.

  4. Between Stage and Screen

    NARCIS (Netherlands)

    Tornqvist, Egil

    1996-01-01

    Ingmar Bergman is worldwide known as a film and stage director. Yet no-one has attempted to compare his stage and screen activities. In Between stage and screen Egil Tornqvist examines formal and thematical correspondences and differences between a number of Bergman's stage, screen, and radio

  5. Screening and evaluation of antiparasitic and in vitro anticancer activities of Panamanian endophytic fungi

    Science.gov (United States)

    Martínez-Luis, Sergio; Cherigo, Lilia; Higginbotham, Sarah; Arnold, Elizabeth; Spadafora, Carmenza; Ibañez, Alicia; Gerwick, William H.; Cubilla-Rios, Luis

    2012-01-01

    Summary Many compounds produced by fungi have relevant pharmaceutical applications. The purpose of this study was to collect and isolate endophytic fungi from different regions of Panama and then to test their potential therapeutic activities against Leishmania donovani, Plasmodium falciparum, and Trypanosoma cruzi as well as their anticancer activities in MCF-7 cells. Of the 25 fungal isolates obtained, ten of them had good anti-parasitic potential, showing selective activity against L. donovani; four had significant anti-malarial activity; and three inhibited the growth of T. cruzi. Anticancer activity was demonstrated in four isolates. Of the active isolates, Edenia sp. strain F0755, Xylaria sp. strain F1220, Aspergillus sp. strain F1544, Mycoleptodiscus sp. strain F0194, Phomopsis sp. strain F1566, Pycnoporus sp. strain F0305, and Diaporthe sp. strain F1647 showed the most promise based on their selective bioactivity and lack of toxicity in the assays. PMID:22069153

  6. Screening of Ficus religiosa leaves fractions for analgesic and anti-inflammatory activities

    OpenAIRE

    Gulecha, Vishal; Sivakumar, T; Upaganlawar, Aman; Mahajan, Manoj; Upasani, Chandrashekhar

    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...

  7. In Silico Screening and In Vitro Activity Measurement of Javamide Analogues as Potential p38 MAPK Inhibitors

    Directory of Open Access Journals (Sweden)

    Jae B. Park

    2017-12-01

    Full Text Available p38 Mitogen-activated protein kinase (p38 MAPK is a protein kinase critically involved in the progress of inflammation/stress-associated diseases. Our data suggested that javamide analogues may contain strong anti-inflammation activities, but there is little information about their effects on p38 MAPK. Therefore, in this paper, the effects of thirty javamide analogues on p38 MAPK were investigated using in silico screening and in vitro p38 MAPK assay methods. The javamide analogues were synthesized and their chemical structures were confirmed using nuclear magnetic resonance (NMR spectroscopic methods. Then, the javamide analogues were screened using an in silico modeling program. The screened analogues demonstrated a wide range of binding energy (ΔE; −20 to −39 and several analogues with ΔE; −34 to −39 showed strong binding affinity to p38 MAPK. In vitro p38 MAPK assay, the kinase was significantly inhibited by the analogues with great binding energy (ΔE; −34 to −39 and in silico scores (Avg. score; −27.5 to −29.3. Furthermore, the comparative analysis of both assays showed a positive correlation between the in silico scores and p38 MAPK inhibition. In fact, the javamide analogues with top five in silico scores (Avg. score; −27.5 to −29.3 were found to inhibit p38 MAPK by 27–31% (p < 0.05 better than those with less scores (ΔE < −27.0. Especially, javamide-II-O-ethyl ester with relatively high in silico score (Avg. score; −29.2 inhibited p38 MAPK (IC50 = 9.9 μM a little better than its methyl ester with best in silico score (Avg. score; −29.3. To support the ability to inhibit p38 MAPK, the treatment of javamide-II-ethyl and -methyl esters could suppress the production of IL-8 and MCP-1 protein significantly by 22–73% (p < 0.05 in the differentiated THP-1 cells, and the inhibition was slightly stronger by the ethyl ester than the methyl ester. Altogether, this study suggests that javamide-II-O-ethyl ester may

  8. Anion-sensitive fluorophore identifies the Drosophila swell-activated chloride channel in a genome-wide RNA interference screen.

    Directory of Open Access Journals (Sweden)

    Stephanie C Stotz

    Full Text Available When cells swell in hypo-osmotic solutions, chloride-selective ion channels (Cl(swell activate to reduce intracellular osmolality and prevent catastrophic cell rupture. Despite intensive efforts to assign a molecular identity to the mammalian Cl(swell channel, it remains unknown. In an unbiased genome-wide RNA interference (RNAi screen of Drosophila cells stably expressing an anion-sensitive fluorescent indicator, we identify Bestrophin 1 (dBest1 as the Drosophila Cl(swell channel. Of the 23 screen hits with mammalian homologs and predicted transmembrane domains, only RNAi specifically targeting dBest1 eliminated the Cl(swell current (I(Clswell. We further demonstrate the essential contribution of dBest1 to Drosophila I(Clswell with the introduction of a human Bestrophin disease-associated mutation (W94C. Overexpression of the W94C construct in Drosophila cells significantly reduced the endogenous I(Clswell. We confirm that exogenous expression of dBest1 alone in human embryonic kidney (HEK293 cells creates a clearly identifiable Drosophila-like I(Clswell. In contrast, activation of mouse Bestrophin 2 (mBest2, the closest mammalian ortholog of dBest1, is swell-insensitive. The first 64 residues of dBest1 conferred swell activation to mBest2. The chimera, however, maintains mBest2-like pore properties, strongly indicating that the Bestrophin protein forms the Cl(swell channel itself rather than functioning as an essential auxiliary subunit. dBest1 is an anion channel clearly responsive to swell; this activation depends upon its N-terminus.

  9. Identification of three classes of heteroaromatic compounds with activity against intracellular Trypanosoma cruzi by chemical library screening.

    Directory of Open Access Journals (Sweden)

    Esther Bettiol

    Full Text Available The development of new drugs against Chagas disease is a priority since the currently available medicines have toxic effects, partial efficacy and are targeted against the acute phase of disease. At present, there is no drug to treat the chronic stage. In this study, we have optimized a whole cell-based assay for high throughput screening of compounds that inhibit infection of mammalian cells by Trypanosoma cruzi trypomastigotes. A 2000-compound chemical library was screened using a recombinant T. cruzi (Tulahuen strain expressing beta-galactosidase. Three hits were selected for their high activity against T. cruzi and low toxicity to host cells in vitro: PCH1, NT1 and CX1 (IC(50: 54, 190 and 23 nM, respectively. Each of these three compounds presents a different mechanism of action on intracellular proliferation of T. cruzi amastigotes. CX1 shows strong trypanocidal activity, an essential characteristic for the development of drugs against the chronic stage of Chagas disease where parasites are found intracellular in a quiescent stage. NT1 has a trypanostatic effect, while PCH1 affects parasite division. The three compounds also show high activity against intracellular T. cruzi from the Y strain and against the related kinetoplastid species Leishmania major and L. amazonensis. Characterization of the anti-T. cruzi activity of molecules chemically related to the three library hits allowed the selection of two compounds with IC(50 values of 2 nM (PCH6 and CX2. These values are approximately 100 times lower than those of the medicines used in patients against T. cruzi. These results provide new candidate molecules for the development of treatments against Chagas disease and leishmaniasis.

  10. Synthesis, Biological Activity and Preliminary in Silico ADMET Screening of Polyamine Conjugates with Bicyclic Systems.

    Science.gov (United States)

    Szumilak, Marta; Galdyszynska, Malgorzata; Dominska, Kamila; Bak-Sypien, Irena I; Merecz-Sadowska, Anna; Stanczak, Andrzej; Karwowski, Boleslaw T; Piastowska-Ciesielska, Agnieszka W

    2017-05-12

    Polyamine conjugates with bicyclic terminal groups including quinazoline, naphthalene, quinoline, coumarine and indole have been obtained and their cytotoxic activity against PC-3, DU-145 and MCF-7 cell lines was evaluated in vitro. Their antiproliferative potential differed markedly and depended on both their chemical structure and the type of cancer cell line. Noncovalent DNA-binding properties of the most active compounds have been examined using ds-DNA thermal melting studies and topo I activity assay. The promising biological activity, DNA intercalative binding mode and favorable drug-like properties of bis(naphthalene-2-carboxamides) make them a good lead for further development of potential anticancer drugs.

  11. Influence of Adiposity, Physical Activity, Fitness, and Screen Time on Insulin Dynamics Over 2 Years in Children.

    Science.gov (United States)

    Henderson, Mélanie; Benedetti, Andrea; Barnett, Tracie A; Mathieu, Marie-Eve; Deladoëy, Johnny; Gray-Donald, Katherine

    2016-03-01

    Despite extensive evidence showing that lifestyle habits play a critical role in preventing or delaying the onset of type 2 diabetes in adults, little is known regarding the impact of lifestyle habits on type 2 diabetes risk in childhood. To assess whether adiposity, fitness, moderate-to-vigorous physical activity, and screen time predict insulin sensitivity or insulin secretion during a 2-year period in children with a family history of obesity. This is a prospective longitudinal cohort study of 630 children, having at least 1 obese parent, recruited from schools in Quebec, Canada, between July 2005 and December 2008 in the Quebec Adipose and Lifestyle Investigation in Youth (QUALITY) cohort. Children were assessed at baseline (ages 8-10 years) and 2 years later. Fitness was measured by peak oxygen consumption, percentage of body fat (adiposity) by dual-energy x-ray absorptiometry, moderate-to-vigorous physical activity using accelerometry, and screen time by average daily hours of self-reported television, video game, or computer use. Regression models were adjusted for age, sex, season, and pubertal stage. The current analysis was completed in October 2015. Insulin sensitivity was measured by the homeostatic model assessment of insulin resistance and an oral glucose tolerance test-based index (Matsuda insulin sensitivity index). Insulin secretion was measured using the area under the curve of insulin to glucose during the first 30 minutes of the oral glucose tolerance test and using the area under the curve of insulin to glucose over 2 hours. Of 630 children evaluated at baseline (mean [SD] age, 9.6 [0.9] years; 54.4% male; 56.2% normal weight, 19.2% overweight, and 22.7% obese), 564 were evaluated at 2-year follow-up. Adiposity and changes in adiposity were the central predictors of insulin dynamics over time. Every additional 1% of body fat at ages 8 to 10 years decreased insulin sensitivity by 2.9% (95% CI, -3.3% to -2.5%; P < .001) and led to a 0.5% (95

  12. Phytochemical screening and biological activity of extracts of plant species Halacsya sendtneri (Boiss. Dörfl.

    Directory of Open Access Journals (Sweden)

    Mašković Pavle Z.

    2012-01-01

    Full Text Available This study is aimed at examining total polyphenol, flavonoid, gallotannin and condensed tannins content in acetone, chloroform, ethyl acetate and petroleum ether extracts of Halacsya sendtneri (Boiss. Dörfl., their antimicrobial and antioxidant activities, as well as identifying and quantifying the phenolic components. The antioxidant activity is consistent with the results of total quantity of phenolic compound. The results showed that the acetone extract of plant species Halascya sendtneri (Boiss. Dörfl. possessed the highest antioxidant activity. IC50 values were determined: 9.45��1.55 μg/mL for DPPH free radical scavenging activity, 13.46±1.68 μg/mL for inhibitory activity against lipid peroxidation, 59.11±0.83 μg/mL for hydroxyl radical scavenging activity and 27.91±0.88 μg/mL for ferrous ion chelating ability. The antimicrobial activity was tested using broth dilution procedure for determination of the minimum inhibitory concentration (MIC. The MICs were determined for 8 selected indicator strains. All of the extracts showed strong to moderate strong antimicrobial activity. The phenolic composition of Halacsya sendtneri extracts was determined by the HPLC method. The dominant phenolic compound in acetone, chloroform and ethyl acetate extract is rosmarinic acid. Ethyl acetate extract was also abundant in p-hydroxybenzoic acid and ferulic acid. The main compounds in petrol ether extract were chlorogenic acid and quercetin.

  13. Anti-diabetic activity-guided screening of aqueous-ethanol Moringa ...

    African Journals Online (AJOL)

    Purpose: To explore the anti-diabetic effects of Moringa oleifera extracts and fractions, and to identify their active/marker compounds. Methods: Five different aqueous ethanol extracts (95, 75, 50, 25 %v/v and 100 % water) of Moringa oleifera were given orally to normal rats to assess their hypoglycemic activities and effect ...

  14. Activity of xenoestrogens at nanomolar concentrations in the E-Screen assay.

    Science.gov (United States)

    Silva, Elisabete; Scholze, Martin; Kortenkamp, Andreas

    2007-12-01

    Certain effects induced by endocrine-disrupting chemicals (EDCs) may occur at dose levels lower than those normally tested in toxicology, but few systematic dose-response studies have been carried out in the low-dose range. The high statistical power afforded by a high-throughput in vitro assay such as the E-Screen assay was exploited with the aim of producing low-dose estimates for 24 estrogenic chemicals, including endogenous hormones and xenoestrogens. Unusual dose-response curves with inverted U-shapes were not observed in the low-dose range. Instead, many chemicals exhibited curves with very small gradients at low doses, and this complicated the reliable estimation of low effects. Systematic comparisons between the outcomes of hypothesis-testing procedures (lowest observed effect concentrations--LOECs, no observed effect concentrations--NOECs) and regression modeling approaches (EC(01)--effective concentration causing a 1% effect, EC(05)--effective concentration causing a 5% effect) produced estimates that agreed reasonably well. In many cases, NOECs were shown to be associated with proliferative responses of 1-2%. This is in contrast with the widespread perception of NOECs as values that signal complete absence of effects. For many of the tested xenoestrogens, the NOECs, EC(01), and EC(05) were in the nanomolar range, and comparisons with measured serum and adipose tissue levels in Europe revealed considerable overlaps in some cases. Our studies illustrate the difficulties that may be encountered during the estimation of low doses in vivo. High statistical power is required when the underlying dose-response curves are shallow. Through the use of large sample sizes and numerous repeats, the experimental power of the E-Screen assay was sufficiently high to measure effect magnitudes of around 1-2% with reliability. However, such resources are usually not available for in vivo testing, with the consequence that the statistical detection limits are considerably

  15. 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.

  16. SCREENING OF 6-PYRUVOYL-TETRAHYDROPTERIN SYNTHASE ACTIVITY DEFICIENCY AMONG HYPERP HENYLALANINEMIC PATIENTS

    Directory of Open Access Journals (Sweden)

    DURDI QUJEQ

    1999-10-01

    Full Text Available A deficiency of the phenylalanine hydroxylase activity or its cofactor tetrahydrobiopterin may"nlead to hyperphenylalamnemia and as a result, loss of IQ, poor school performance, and"nbehavior problems occurs. Deficiency in 6-pyruvoyl-tetrahydropterin synthase activity is the"nmajor cause of tetrahydrobiopterin deficient phenylketonuria. In this study, blood specimens"nfrom 165 healthy volunteers and 127 children with phenylketonuria were used to determine"nthe 6-pyruvoyl-tetrahydropterin synthase activity. It was found that the activity of 6-"npyruvoyl- tetrahydropterin synthase was decreased in comparison with control [23.46 +/-"n2.94, (mean +/- SD, mmol/ ml/h, n=I27 vs. 127.63 +/- 4.52, n=165, p<0.05]. Results of"nthis study indicate that examination of 6-pyruvoyl-tetrahydropterin synthase activity is helpful"nand may lead to the diagnosis cause of hyperphenylalaninemia.

  17. Screening and evaluation of active compounds in polyphenol mixtures by HPLC coupled with chemical methodology and its application.

    Science.gov (United States)

    Zhao, Yue; Wang, Ying; Jiang, Zi-Tao; Li, Rong

    2017-07-15

    An off-line high performance liquid chromatography (HPLC) coupled with chemical methods has been developed to evaluate antioxidant activity of 11 standard polyphenol compounds (SPCs) and vitamin C (Vc) in terms of radical scavenging abilities. The structure-activity relationships of each SPC were also discussed. SPCs showed different abilities in scavenging 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azinobis-3-ethyl-benzthiazoline-6-sulphonate (ABTS + ) and hydroxyl (OH) free radicals. Among SPCs, quercetin and kaempferol, as typical flavonoids, displayed the greatest radical-scavenging activities and even exhibited higher activity in OH radical removal ability than that of Vc. Furthermore, the proposed method was also applied to screening polyphenolic antioxidant components from Cichorium endivia L. (C. endivia) seed extract. The results indicated that cynarin in the extract was a more active compound to scavenge DPPH and ABTS + radicals than chlorogenic acid, while chlorogenic acid had stronger capacity in scavenging OH free radicals. Copyright © 2017 Elsevier Ltd. All rights reserved.

  18. Actinomycetes from solitary wasp mud nest and swallow bird mud nest: isolation and screening for their antibacterial activity.

    Science.gov (United States)

    Kumar, Vijay; Bharti, Alpana; Gupta, Vivek Kumar; Gusain, Omprakash; Bisht, Gajraj Singh

    2012-03-01

    The aim of this study was to isolate and screen actinomycetes from solitary wasp and swallow bird mud nests for antimicrobial activity. The actinomycetes were isolated from soil of nests of solitary wasp and swallow bird, and identified on the basis of morphological characteristics and molecular biological methods. A total of 109 actinomycetal isolates were obtained from 12 soil samples (6 from each habitat) using two media. The highest number of actinomycetes were recovered on Humic acid vitamin agar media (65.13%, n = 71) as compared to actinomycetes isolation agar media (34.86%, n = 38). The antimicrobial activity of actinomycetes isolates was determined using the agar plug method. Among 109 isolates, 51 isolates (46.78%) showed antibacterial activity by agar plug assay. The morphological and molecular characteristics confirmed that the most of active isolates in both sample belonged to the genus Streptomyces, the other potential genera like Streptosporangium, Actinomadura, Saccharopolyspora, Thermoactinomycetes and Nocardia were also recovered, but in a low frequency. The isolates designated as 8(1), BN-6, MN 2(6), MN 2(7) and MN 9(V) showed most promising activity against various drug resistant bacterial pathogens. It seems that the promising isolates from these unusual/unexplored habitats may prove to be an important step in development of drug for treating multi-drug resistant bacterial pathogens.

  19. Tartrazine and sunset yellow are xenoestrogens in a new screening assay to identify modulators of human oestrogen receptor transcriptional activity

    International Nuclear Information System (INIS)

    Axon, Andrew; May, Felicity E.B.; Gaughan, Luke E.; Williams, Faith M.; Blain, Peter G.; Wright, Matthew C.

    2012-01-01

    Primary biliary cirrhosis (PBC) is a cholestatic liver disease of unknown cause that occurs most frequently in post-menopausal women. Since the female sex hormone oestrogen can be cholestatic, we hypothesised that PBC may be triggered in part by chronic exposure to xenoestrogens (which may be more active on a background of low endogenous oestrogen levels seen in post-menopausal women). A reporter gene construct employing a synthetic oestrogen response element predicted to specifically interact with oestrogen receptors (ER) was constructed. Co-transfection of this reporter into an ER null cell line with a variety of nuclear receptor expression constructs indicated that the reporter gene was trans-activated by ERα and ERβ, but not by the androgen, thyroid, progesterone, glucocorticoid or vitamin D receptors. Chemicals linked to PBC were then screened for xenoestrogen activity in the human ERα-positive MCF-7 breast cancer cell line. Using this assay, the coal-derived food and cosmetic colourings – sunset yellow and tartrazine – were identified as novel human ERα activators, activating the human ER with an EC 50% concentration of 220 and 160 nM, respectively.

  20. Tartrazine and sunset yellow are xenoestrogens in a new screening assay to identify modulators of human oestrogen receptor transcriptional activity.

    Science.gov (United States)

    Axon, Andrew; May, Felicity E B; Gaughan, Luke E; Williams, Faith M; Blain, Peter G; Wright, Matthew C

    2012-08-16

    Primary biliary cirrhosis (PBC) is a cholestatic liver disease of unknown cause that occurs most frequently in post-menopausal women. Since the female sex hormone oestrogen can be cholestatic, we hypothesised that PBC may be triggered in part by chronic exposure to xenoestrogens (which may be more active on a background of low endogenous oestrogen levels seen in post-menopausal women). A reporter gene construct employing a synthetic oestrogen response element predicted to specifically interact with oestrogen receptors (ER) was constructed. Co-transfection of this reporter into an ER null cell line with a variety of nuclear receptor expression constructs indicated that the reporter gene was trans-activated by ERα and ERβ, but not by the androgen, thyroid, progesterone, glucocorticoid or vitamin D receptors. Chemicals linked to PBC were then screened for xenoestrogen activity in the human ERα-positive MCF-7 breast cancer cell line. Using this assay, the coal-derived food and cosmetic colourings--sunset yellow and tartrazine--were identified as novel human ERα activators, activating the human ER with an EC(50%) concentration of 220 and 160 nM, respectively. Copyright © 2012 Elsevier Ireland Ltd. All rights reserved.

  1. The in vitro screening for acetylcholinesterase inhibition and antioxidant activity of medicinal plants from Portugal.

    Science.gov (United States)

    Ferreira, A; Proença, C; Serralheiro, M L M; Araújo, M E M

    2006-11-03

    Essential oil, ethanolic extract and decoction of 10 plant species from interior Portugal were analyzed for their activity towards acetylcholinesterase (AChE) enzyme and their antioxidant activity. Of these, Melissa officinalis, Paronychia argentea, Sanguisorba minor, Hypericum undulatum and Malva silvestris are used in herbal medicine, Laurus nobilis and Mentha suaveolens as condiments, and Salvia officinalis, Lavandula angustifolia and Lavandula pedunculata also as aromatics. Melissa officinalis and Mentha suaveolens showed AChE inhibitory capacity higher then 50% in the essential oil fraction. Laurus nobilis, Hypericum undulatum, and Sanguisorba minor showed a high inhibition value of AChE in the ethanolic fraction, 64% (1 mg ml(-1)) 68% (0.5 mg ml(-1)), and 78% (1 mg ml(-1)), respectively. Higher values of AChE inhibitory activity were found using decoctions of Lavandula pedunculata, Mentha suaveolens and Hypericum undulatum, 68, 69 and 82% (at a concentration of 5mg dry plant ml(-1) of assay), respectively. The free radical scavenger activity was higher for the polar extracts. In the water extracts most of the plants showed values around 90%. When antioxidant activity was measured with the beta-carotene-linoleic acid assay high activity (65-95%) was also found in the water extracts. Hypericum undulatum, Melissa officinalis and Laurus nobilis showed both high AChE inhibitory capacity and antioxidant activity.

  2. Location performance objectives for the NNWSI area-to-location screening activity

    International Nuclear Information System (INIS)

    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

  3. 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.

  4. 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.

    2016-01-01

    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

  5. 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.

  6. 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

  7. Screening of the anticonvulsant activity of some plants from Fabaceae family in experimental seizure models in mice

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    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.

  8. Screening single-atom catalysts for methane activation: α -A l2O3(0001 ) -supported Ni

    Science.gov (United States)

    Gao, Fei; Gao, Shiwu; Meng, Sheng

    2017-08-01

    Methane activation is one of the biggest challenges for chemical conversion of hydrocarbons and fundamental science. We systematically screen d -block transition metal elements as potential candidates of single-atom catalysts (SACs) for methane dissociation. The adsorption of methane on free metal atoms strongly depends on the number of d electrons of SAC, where the maximum binding energy is formed with the Ni group (electronic configuration d8s2 or d9s1 ). Interestingly, the magnetic moment of the SACs decreases by 2 μB for strong interactions, suggesting that the methane-metal bond forms a spin singlet state involving two electrons of opposite spins. To examine the effect of substrates, the screened transition metals, Ni, Rh, and Pt are further put onto prototype metal oxide surfaces. The substrate dramatically modifies the discrete energy levels of a single metal and its catalytic properties. Single Ni atoms supported on an O-terminated α -A l2O3(0001 ) surface (N i1/A l2O3 ) show superior catalytic properties, with a low activation barrier of 0.4 eV (0.11 eV after zero-point energy correction) for the C-H bond dissociation and simultaneously an extreme stability with a high binding energy of ˜9.39 eV for the Ni anchor. This work identifies N i1/A l2O3 catalyst as an optimal SAC and offers new atomistic insights into the mechanism of methane activation on SACs.

  9. A high throughput gas exchange screen for determining rates of photorespiration or regulation of C4 activity.

    Science.gov (United States)

    Bellasio, Chandra; Burgess, Steven J; Griffiths, Howard; Hibberd, Julian M

    2014-07-01

    Large-scale research programmes seeking to characterize the C4 pathway have a requirement for a simple, high throughput screen that quantifies photorespiratory activity in C3 and C4 model systems. At present, approaches rely on model-fitting to assimilatory responses (A/C i curves, PSII quantum yield) or real-time carbon isotope discrimination, which are complicated and time-consuming. Here we present a method, and the associated theory, to determine the effectiveness of the C4 carboxylation, carbon concentration mechanism (CCM) by assessing the responsiveness of V O/V C, the ratio of RuBisCO oxygenase to carboxylase activity, upon transfer to low O2. This determination compares concurrent gas exchange and pulse-modulated chlorophyll fluorescence under ambient and low O2, using widely available equipment. Run time for the procedure can take as little as 6 minutes if plants are pre-adapted. The responsiveness of V O/V C is derived for typical C3 (tobacco, rice, wheat) and C4 (maize, Miscanthus, cleome) plants, and compared with full C3 and C4 model systems. We also undertake sensitivity analyses to determine the impact of R LIGHT (respiration in the light) and the effectiveness of the light saturating pulse used by fluorescence systems. The results show that the method can readily resolve variations in photorespiratory activity between C3 and C4 plants and could be used to rapidly screen large numbers of mutants or transformants in high throughput studies. © The Author 2014. Published by Oxford University Press on behalf of the Society for Experimental Biology.

  10. Validation of the AlamarBlue® assay as a fast screening method to determine the antimicrobial activity of botanical extracts

    OpenAIRE

    Tyc, O.; Tomás-Menor, L.; Garbeva, P.V.; Barrajón-Catalán, E.; Micol, V.

    2016-01-01

    Plant compounds are a potential source of new antimicrobial molecules against a variety of infections. Plant extracts suppose complex phytochemical libraries that may be used for the first stages of the screening process for antimicrobials. However, their large variability and complexity require fast and inexpensive methods that allow a rapid and adequate screening for antimicrobial activity against a variety of bacteria and fungi. In this study, a multi-well plate assay using the AlamarBlue®...

  11. 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...

  12. Isolation of Mucorales from processed maize (Zea mays L.) and screening for protease activity

    OpenAIRE

    de Azevedo Santiago, Andr? Luiz Cabral Monteiro; de Souza Motta, Cristina Maria

    2008-01-01

    Mucorales were isolated from maize flour, corn meal and cooked cornflakes using surface and depth plate methods. Rhizopus oryzae, Circinella muscae, Mucor subtilissimus, Mucor hiemalis f. hiemalis, Syncephalastrum racemosum, Rhizopus microsporus var. chinensis and Absidia cylindrospora showed protease activity.

  13. In vitro screening of methanol plant extracts for their antibacterial activity

    International Nuclear Information System (INIS)

    Hussain, T.; Arshad, M.; Khan, S.; Sattar, H.

    2011-01-01

    The purpose of this study was to observe the antibacterial activity of aqueous methanolic extracts of 10 plants against 2-gram negative bacteria (Pasteurella multocida, Escherichia coli) and 3-gram positive bacteria (Bacillus cereus, Staphylococcus aureus, Corynebacterium bovis) by using disc diffusion method. The minimum inhibitory concentration (MIC) was determined by agar well diffusion method and agar dilution method. All the bacteria were susceptible to different plant extracts. Lawsonia inermis, Embellia ribes and Santalum album showed antibacterial activity against all the tested bacteria. The extract of Santalum album showed maximum antibacterial activity of the 10 plant extracts used. Bacillus cereus and Pasteurella multocida were the most sensitive bacteria against most of the plant extracts. It is clear from the results of the present studies that the plant extracts have great potential as antimicrobial compounds against bacteria. However, there is a need of further research to isolate the active ingredients for further pharmacological evaluation. (author)

  14. In vitro screening for potential chemical inhibitors of deiodinase type 1 activity

    Science.gov (United States)

    Control of thyroid hormone (TH) signaling in vertebrates is dependent upon multiple key events including iodide uptake, hormone synthesis, metabolism and elimination, to maintain proper homeostasis of the hormones. Deiodinase enzymes interconvert THs between less active and more...

  15. Body image dissatisfaction, physical activity and screen-time in Spanish adolescents.

    Science.gov (United States)

    Añez, Elizabeth; Fornieles-Deu, Albert; Fauquet-Ars, Jordi; López-Guimerà, Gemma; Puntí-Vidal, Joaquim; Sánchez-Carracedo, David

    2018-01-01

    This cross-sectional study contributes to the literature on whether body dissatisfaction is a barrier/facilitator to engaging in physical activity and to investigate the impact of mass-media messages via computer-time on body dissatisfaction. High-school students ( N = 1501) reported their physical activity, computer-time (homework/leisure) and body dissatisfaction. Researchers measured students' weight and height. Analyses revealed that body dissatisfaction was negatively associated with physical activity on both genders, whereas computer-time was associated only with girls' body dissatisfaction. Specifically, as computer-homework increased, body dissatisfaction decreased; as computer-leisure increased, body dissatisfaction increased. Weight-related interventions should improve body image and physical activity simultaneously, while critical consumption of mass-media interventions should include a computer component.

  16. Screening of antibacterial and antifungal activities of selected Macedonian wild mushrooms

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    Nikolovska-Nedelkoska Daniela

    2013-01-01

    Full Text Available Regarding the development of novel safe antimicrobials of natural origin, macrofungi became attractive for the researchers in the last decade. In this study, antimicrobial potential of methanolic extracts of six wild macromycetes (Boletus lupinus, Flammulina velutypes, Phellinus igniarius, Sarcodon imbricatus, Tricholoma aurantium, Xerocomus ichnusanus was evaluated. In vitro antimicrobial activity was investigated by the microdilution method and minimum inhibitory concentration (MIC was determined. Testing was conducted against eleven microorganisms, including six strains of bacteria and five species of fungi. Extracts showed selective antimicrobial properties while the activities depended both on the species of m